Saunders Nursing Drug Handbook 2021 1nbsped 9780323757287 0323757286 9780323757294 0323757294 204 1528

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abacavir/dolutegravir/lamivudine 1

A
s­ubstitutions or clinically suspected inte-
abacavir/ grase strand transfer inhibitor resistance;
dolutegravir/ creatinine clearance less than 50 mL/min;
mild hepatic impairment; children weigh-
lamivudine ing less than 40 kg.

a-bak-a-veer/doe-loo-teg-ra-vir/la- ACTION
miv-yoo-deen Abacavir interferes with HIV viral RNA-
(Triumeq) dependent DNA polymerase. Dolutegravir
j BLACK BOX ALERT jSerious, inhibits HIV integrase by blocking strand
sometimes fatal hypersensitivity transfer step of retroviral DNA integra-
reactions, lactic acidosis, severe he- tion (essential for HIV replication cycle).
patomegaly with steatosis (fatty liver) Lamivudine inhibits reverse transcriptase
have occurred with abacavir-contain-
ing products, esp. in pts who carry by viral DNA chain termination. Thera-
the HLA-B*5701 allele. Restarting peutic Effect: Interferes with HIV
abacavir following a hypersensitivity replication, slowing progression of HIV
reaction may be life-threatening. May infection.
cause hepatitis B virus reactivation.
Do not confuse abacavir with PHARMACOKINETICS
entercavir, or dolutegravir with Abacavir, lamivudine rapidly absorbed
elvitegravir or raltegravir, or and widely distributed. Abacavir distrib-
lamivudine with telbivudine or utes into cerebrospinal fluid (CSF) and
lamotrigine. erythrocytes. Abacavir metabolized by
alcohol dehydrogenase and glucuronyl
FIXED-COMBINATION(S) transferase. Dolutegravir metabolized in
abacavir/dolutegravir/lamivudine (an- liver. Protein binding: abacavir: 50%; do-
tiretrovirals): 600 mg/50 mg/300 mg. lutegravir: 98.9%; lamivudine: less than
uCLASSIFICATION
36%. Peak plasma concentration: dolute-
gravir: 2–3 hrs. Excretion: abacavir: urine
PHARMACOTHERAPEUTIC: Inte- (primary); dolutegravir: feces (53%),
grase inhibitor (INSTI), Reverse urine (31%); lamivudine: urine (70%).
Transcriptase inhibitor, Nucleoside. Half-life: abacavir: 1.5 hrs; dolutegra-
CLINICAL: Antiretroviral. vir: 14 hrs; lamivudine: 5–7 hrs.

USES LIFESPAN CONSIDERATIONS


Treatment of HIV-1 infection, in adults and Pregnancy/Lactation: Breastfeed-
children weighing at least 40 kg. ing not recommended due to risk of
postnatal HIV transmission. Unknown
PRECAUTIONS if distributed in breast milk. Chil-
Contraindications: Hypersensitivity to aba­ dren: Safety and efficacy not estab-
cavir, dolutegravir, lamivudine. Pts who test lished in pts weighing less than 40 kg.
positive for the HLA-B*5701 allele. Con- Elderly: May have increased risk of
comitant use of dofetilide. Pts with mod- adverse effects; worsening of hepatic,
erate to severe hepatic impairment. Cau- renal, cardiac function.
tions: Diabetes, hepatic/renal impairment,
coronary artery disease, history of hepatitis INTERACTIONS
or tuberculosis, prior hypersensitivity reac- DRUG: Dolutegravir may increase con-
tion to INSTIs. Use in children with history centration/effect of dofetilide (contra-
of pancreatitis or risk factors for develop- indicated). Fosphenytoin, phenytoin,
ing pancreatitis. Not ­ recommended in nevirapine, o­ xcarbazepine, phe-
pts with resistance-associated integrase nobarbital, primidone may decrease
Canadian trade name Non-Crushable Drug High Alert drug
2 abacavir/dolutegravir/lamivudine
A
c­ oncentration of dolutegravir. Lamivudine intractable nausea/vomiting, multi-organ
may increase adverse/toxic effects of em- failure, pharyngitis may occur within the
tricitabine. HERBAL: St. John’s wort may first 6 wks of treatment with abacavir (8%
decrease effect of dolutegravir. FOOD: None of pts). If therapy is discontinued, pts co-
known. LAB VALUES: May increase serum infected with hepatitis B or C virus have
amylase, ALT, AST, bilirubin, cholesterol, an increased risk for viral replication,
creatine kinase (CK), creatinine, glucose, worsening of hepatic function, and may
lipase, triglycerides. May decrease Hgb, experience hepatic decompensation and/
Hct, neutrophils. or failure. May induce immune recovery
syndrome (inflammatory response to
AVAILABILITY (Rx) dormant opportunistic infections such
abacavir
Fixed-Dose Combination Tablet: as Mycobacterium avium, cytomegalovi-
600 mg/dolutegravir 50 mg/lamivudine rus, PCP, tuberculosis, or acceleration of
300 mg. autoimmune disorders such as Graves’
disease, polymyositis, Guillain-Barré).
ADMINISTRATION/HANDLING Fatal cases of lactic acidosis, severe
PO hepatomegaly with steatosis have been
• Give without regard to food. • Admin- reported. Hepatic failure occurred in
ister at least 2 hrs before or at least 6 hrs 1% of pts taking dolutegravir-containing
after giving medications containing alumi- products. Abacavir-containing products
num, calcium, iron, magnesium (supple- may increase risk of myocardial infarc-
ments, antacids, laxatives). tion, erythema multiform, Stevens-John-
son Syndrome, toxic epidermal necroly-
INDICATIONS/ROUTES/DOSAGE sis. May increase risk of pancreatitis.
HIV Infection
PO: ADULTS, ELDERLY, CHILDREN WEIGHING
NURSING CONSIDERATIONS
40 KG OR MORE: 1 tablet once daily. BASELINE ASSESSMENT

Dosage in Renal Impairment Obtain CBC, BMP, LFT, CD4+ count, vi-
Creatinine clearance less than 50 mL/ ral load, HIV-1 RNA level. Obtain weight
min: Not recommended. in kilograms. Screen for HLA-B* 5701
allele, hepatitis B or C virus infection
Dosage in Hepatic Impairment before initiating therapy. Question for
Mild impairment: Consider use of indi- prior hypersensitivity reactions (espe-
vidual components. Moderate to severe cially to abacavir-containing products);
impairment: Contraindicated. history of diabetes, coronary artery dis-
ease, hepatic/renal impairment. Receive
SIDE EFFECTS full medication history, including herbal
Rare (3%–1%): Insomnia, fatigue, head- products. Question possibility of preg-
ache, abdominal pain/distension, dys- nancy. Offer emotional support.
pepsia, flatulence, gastroesophageal INTERVENTION/EVALUATION
reflux disease, fever, lethargy, anorexia,
arthralgia, myositis, somnolence, pruri- Monitor CBC, BMP, LFT periodically. Im-
tus, depression, abnormal dreams, dizzi- mediately discontinue if hypersensitivity
ness, nausea, diarrhea, rash. reaction is suspected, even when other
diagnoses are possible (e.g., pneumo-
ADVERSE EFFECTS/ nia, bronchitis, pharyngitis, influenza,
TOXIC REACTIONS gastroenteritis, reactions to other medi-
cations). Stop treatment if 3 or more of
Serious and sometimes fatal hypersen- the following symptoms occur: rash, fe-
sitivity reactions including anaphylaxis, ver, GI disturbances (diarrhea, nausea,
severe diarrhea, dyspnea, hypotension,
underlined – top prescribed drug
abaloparatide 3
A
vomiting), flu-like symptoms, respiratory
distress. If hypersensitivity reaction is re- abaloparatide
lated to abacavir, do not restart treatment
(may cause more severe reactions and/ a-bal-oh-par-a-tide
or death within hours). Assess for he- (Tymlos)
patic impairment (bruising, hematuria,
jaundice, right upper abdominal pain, j BLACK BOX ALERT jMay
cause a dose-dependent increase
nausea, vomiting, weight loss). Screen in the incidence of osteosarcoma. It
for immune recovery syndrome, rhab- is unknown whether abaloparatide
domyolysis (muscle weakness, myalgia, will cause osteosarcoma in humans.
decreased urinary output). Pediatric pts Avoid use in pts at risk for osteosar-
should be closely monitored for symp- coma (e.g., pts with Paget’s disease
of bone or unexplained elevations of
toms of pancreatitis (severe, steady ab- alkaline phosphatase, pediatric and
dominal pain often radiating to the back; young adults with open epiphyses,
clammy skin, reduced B/P; nausea and pts with bone metastasis or skeletal
vomiting accompanied by abdominal malignancies, hereditary disorders
pain). Monitor daily stool pattern, con- predisposing to osteosarcoma, or
prior history of external beam or
sistency; I&Os. Assess dietary pattern; implant radiation involving the skel-
monitor for weight loss. Screen for toxic eton. Cumulative use of parathyroid
skin reactions. Monitor for symptoms of analogs (e.g., teriparatide) for more
MI (jaw/chest/left arm pain or pressure, than 2 yrs during a pt’s lifetime is not
dyspnea, diaphoresis, vomiting). recommended.
Do not confuse abaloparatide
PATIENT/FAMILY TEACHING with teriparatide.
• Blood levels will be monitored periodi-
cally. • Treatment does not cure HIV in- uCLASSIFICATION
fection nor reduce risk of transmission.
Practice safe sex with barrier methods or PHARMACOTHERAPEUTIC: Para-
abstinence. • As immune system strength- thyroid hormone receptor analog.
CLINICAL: Osteoporosis agent.
ens, it may respond to dormant infections
hidden within the body. Report any new fe-
ver, chills, body aches, cough, night sweats, USES
shortness of breath. • Antiretrovirals may Treatment of postmenopausal women
cause excess body fat in upper back, neck, with osteoporosis at high risk for frac-
breast, trunk; may cause decreased body fat ture, defined as history of osteoporotic
in legs, arms, face. • Drug resistance can fracture, multiple risk factors for frac-
form if therapy is interrupted for even a ture, or pts who have failed or are intol-
short time; do not run out of supply. • Re- erant to other osteoporosis therapy.
port signs of abdominal pain, darkened
urine, decreased urine output, yellowing of PRECAUTIONS
skin or eyes, clay colored stools, weight Contraindications: Hypersensitivity to
loss. • Do not breastfeed. • Small, fre- abaloparatide. Cautions: Pts at risk for
quent meals may offset anorexia, nau- hypercalcemia (e.g., hyperparathyroid-
sea. • Take dose at least 2 hrs before or ism, renal impairment, severe dehydra-
at least 6 hrs after other medications con- tion; history of hypercalciuria, urolithia-
taining aluminum, calcium, iron, magne- sis). Avoid use in pts at increased risk for
sium (supplements, antacids, laxa- osteosarcoma (e.g., pts with Paget’s dis-
tives). • Do not take newly prescribed ease of bone or unexplained elevations
medications, including OTC drugs, unless of alkaline phosphatase, open epiphyses,
approved by doctor who originally started bone or skeletal malignancies, hereditary
treatment. disorders predisposing to osteosarcoma,
Canadian trade name Non-Crushable Drug High Alert drug
4 abaloparatide
A
prior radiation therapy involving the psoriasis. • Do not administer IV or
skeleton). Not recommended in pts with intramuscularly. • Rotate injection sites.
cumulative use of parathyroid analogs Storage • Refrigerate unused injector
greater than 2 yrs during lifetime. pens. • After first use, store at room
temperature for up to 30 days. • Do
ACTION not freeze or expose to heating sources.
Acts as an agonist at the PTH1 receptor.
Therapeutic Effect: Stimulates osteo- INDICATIONS/ROUTES/DOSAGE
blast function and increases bone mass, Postmenopausal Osteoporosis
decreasing risk of fractures. SQ: ADULTS, ELDERLY: 80 mcg once daily.
Give with supplemental calcium and vita-
PHARMACOKINETICS min D if dietary intake is inadequate.
Widely distributed. Metabolism not speci-
fied. Degraded into small peptides via Dosage in Renal Impairment
proteolytic enzymes. Protein binding: 70%. No dose adjustment.
Peak plasma concentration: 0.51 hrs. Ex- Dosage in Hepatic Impairment
creted primarily in urine. Not expected to Not specified; use caution.
be removed by dialysis. Half-life: 1.7 hrs.
SIDE EFFECTS
LIFESPAN CONSIDERATIONS
Frequent (58%): Injection site reactions
Pregnancy/Lactation: Not indicated (edema, pain, redness). Occasional
in females of reproductive potential. (10%–5%): Dizziness, nausea, headache,
Unknown if distributed in breast milk or palpitations. Rare (3%–2%): Fatigue, up-
crosses the placenta. Children: Safety per abdominal pain, vertigo.
and efficacy not established. Elderly: No
age-related precautions noted. ADVERSE EFFECTS/TOXIC
REACTIONS
INTERACTIONS
May increase risk of osteosarcoma.
DRUG: None known. HERBAL: None sig- Hypercalcemia reported in 3% of pts.
nificant. FOOD: None known. LAB VAL- Tachycardia occurred in 2% of pts (usu-
UES: May increase serum calcium, uric ally within 15 min after injection). Or-
acid; urine calcium. thostatic hypotension reported in 4% of
AVAILABILITY (Rx) pts (usually within 4 hrs after injection).
Hypercalciuria and urolithiasis reported
3120 mcg/1.56
Prefilled Injector Pens: in 20% and 2% of pts, respectively. Im-
mL (2000 mcg/mL). Delivers 30 doses munogenicity (auto-abaloparatide anti-
of 80 mcg. bodies) occurred in 49% of pts.
ADMINISTRATION/HANDLING NURSING CONSIDERATIONS
SQ
• Visually inspect for particulate matter BASELINE ASSESSMENT
or discoloration. Solution should appear Obtain baseline parathyroid hormone
clear, colorless. • Do not use if solution level. Screen for risk of osteosarcoma,
is cloudy, discolored, or if visible particles hypercalcemia (as listed in Precautions);
are observed. • Insert needle subcuta- prior use of parathyroid analogs. Assess
neously into the periumbilical region of pt’s willingness to self-inject medication.
the abdomen (avoid a 2-inch area around
the navel) and inject solution. • Do not INTERVENTION/EVALUATION
inject into areas of active skin disease or Monitor bone mineral density, para-
injury such as sunburns, skin rashes, thyroid hormone level; serum calcium.
inflammation, skin infections, or active
­ Monitor urinary calcium levels, esp. in

underlined – top prescribed drug


abatacept 5
A
pts with preexisting hypercalciuria or methotrexate. Treatment of active adult
­active urolithiasis. Due to risk of ortho- psoriatic arthritis. Treatment of moderate
static hypotension, administer the first to severe active polyarticular juvenile idio-
several doses with the pt in the lying or pathic arthritis in pts 2 yrs and older. May
sitting position. Monitor for orthostatic use alone or in combination with metho-
hypotension (dizziness, palpitations, trexate. Note: Do not use with anakinra or
tachycardia, nausea, syncope). If ortho- tumor necrosis factor [TNF] antagonists.
static hypotension occurs, place pt in
supine position. Assess need for calcium, PRECAUTIONS
vitamin D supplementation. Contraindications: Hypersensitivity to
abatacept. Cautions: Chronic, latent, or
PATIENT/FAMILY TEACHING localized infection; conditions predispos-
• Receive the first several injections while ing to infections (diabetes, indwelling
lying or sitting down. Slowly go from lying catheters, renal failure, open wounds);
to standing to avoid an unusual drop in COPD (higher incidence of adverse ef-
blood pressure. Immediately sit or lie fects); elderly, hx recurrent infections.
down if dizziness, near-fainting, palpita-
tions occur. • Report symptoms of high ACTION
calcium levels (e.g., constipation, lethargy, Inhibits T-cell (T-lymphocyte) activation.
nausea, vomiting, weakness); severe bone Activated T-cells are found in synovium of
pain. • An increased heart rate may oc- rheumatoid arthritic patients. Therapeutic
cur after injection and will usually subside Effect: Induces positive clinical response
within 6 hrs. • A healthcare provider in adult pts with moderate to severely active
will show you how to properly prepare RA or juvenile idiopathic arthritis.
and inject your medication. You must
demonstrate correct preparation and in- PHARMACOKINETICS
jection techniques before using medica- Higher clearance with increasing body
tion at home. • Vitamin D and calcium weight. Age, gender do not affect clear-
supplementation may be required if di- ance. Half-life: 8–25 days.
etary intake is inadequate.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses pla-
abatacept centa; unknown if distributed in breast
milk. Children: Safety and efficacy not
a-bay-ta-sept established in pts younger than 6 yrs.
(Orencia) Elderly: Cautious use due to increased
Do not confuse Orencia, Orencia risk of serious infection and malignancy.
ClickJect
INTERACTIONS
uCLASSIFICATION DRUG: Anakinra, anti-TNF agents,
PHARMACOTHERAPEUTIC: Selective baricitinib, pimecrolimus, ritux-
T-cell costimulation modulator. imab, tacrolimus (topical), tocili-
CLINI­­CAL: Antirheumatic: disease zumab may increase adverse effects.
modifying. May decrease therapeutic effect of BCG
(intravesical), vaccines (live). May
increase concentration/effect of beli-
USES mumab, natalizumab, tofacitinib,
Reduction of signs and symptoms, pro- vaccines (live). HERBAL: Echinacea
gression of structural damage in adults may decrease concentration/effects.
with moderate to severe rheumatoid ar- FOOD: None known. LAB VALUES: None
thritis (RA) alone or in combination with significant.

Canadian trade name Non-Crushable Drug High Alert drug


6 abatacept
A
AVAILABILITY (Rx) rub injection site. • Rotate injection
IV Injection, Powder for Reconstitu- sites.
tion: 250 mg. SQ Injection, Solution:
IV INCOMPATIBILITIES
50 mg/0.4 mL, 87.5 mg/0.7 mL, 125 mg/
mL single-dose prefilled syringe. Do not infuse concurrently in same IV
line as other agents.
ADMINISTRATION/HANDLING
INDICATIONS/ROUTES/DOSAGE
IV Note: Discontinue in pts developing se-
Reconstitution • Reconstitute each rious infection.
vial with 10 mL Sterile Water for Injec- Rheumatoid Arthritis (RA), Psoriatic
tion using the silicone-free syringe pro- Arthritis (PsA)
vided with each vial and an 18- to IV: ADULTS, ELDERLY WEIGHING 101 KG OR
21-gauge needle. • Rotate solution MORE: 1 g (4 vials) given as a 30-min
gently to prevent foaming until powder infusion. Following initial therapy, give
is completely dissolved. • From a at 2 wks and 4 wks after first infusion,
100-mL 0.9% NaCl infusion bag, with- then q4wks thereafter. WEIGHING 60–100
draw and discard an amount equal to KG: 750 mg (3 vials) given as a 30-min
the volume of the reconstituted vials infusion. Following initial therapy, give
(for 2 vials remove 20 mL, for 3 vials at 2 wks and 4 wks after first infusion,
remove 30 mL, for 4 vials remove then q4wks thereafter. WEIGHING 59 KG OR
40 mL), resulting in final volume of LESS: 500 mg (2 vials) given as a 30-min
100 mL. • Slowly add the reconsti- infusion. Following initial therapy, give at
tuted solution from each vial into the 2 wks and 4 wks after first infusion, then
infusion bag using the same syringe q4wks thereafter.
provided with each vial. • Concentra- SQ: (RA): Following a single IV infusion,
tion in the infusion bag will be 10 mg/ 125 mg given within 24 hrs of infusion,
mL or less abatacept. then 125 mg once a week (SQ admin-
Rate of administration • Infuse over istration may be initiated without an IV
30 min using a 0.2 to 1.2 micron low loading dose). (PsA): Give without an
protein-binding filter. IV loading dose. 125 mg once weekly.
Storage • Store vials, prefilled sy- Transitioning from IV to SQ: Give
ringes in refrigerator. • Any reconstitu- 1st SQ dose instead of next scheduled IV
tion that has been prepared by using sili- dose.
conized syringes will develop translucent
particles and must be discarded. • So- Juvenile Idiopathic Arthritis
lution should appear clear and colorless Note: Dose based on body weight at each
to pale yellow. Discard if solution is administration.
discolored or contains precipitate. IV: CHILDREN 6 YRS AND OLDER, WEIGH-
• Solution is stable for up to 24 hrs after ING LESS THAN 75 KG: 10 mg/kg.
reconstitution. • Reconstituted solution CHILDREN WEIGHING 75–100 KG: 750
may be stored at room temperature or mg. WEIGHING MORE THAN 100 KG: 1,000
refrigerated. mg. Following initial therapy, give 2
wks and 4 wks after first infusion, then
SQ q4wks thereafter.
• Allow syringe to warm to room tem- SQ: CHILDREN 2 YRS AND OLDER, ADO-
perature (30–60 min). • Inject in front LESCENTS WEIGHING 50 KG OR MORE: 125
of thigh, outer areas of upper arms, or mg once weekly. WEIGHING 25–49 KG:
abdomen. • Avoid areas that are tender, 87.5 mg once weekly. WEIGHING 10–24
bruised, red, scaly, or hard. • Do not KG: 50 mg once weekly.

underlined – top prescribed drug


abemaciclib 7
A
Dosage Adjustment for Toxicity
Discontinue in pts developing a serious abemaciclib
infection.
a-bem-a-sye-klib
Dosage in Renal/Hepatic Impairment (Verzenio)
No dose adjustment. Do not confuse abemaciclib with
palbociclib or ribociclib.
SIDE EFFECTS uCLASSIFICATION
Frequent (18%): Headache. Occasional
PHARMACOTHERAPEUTIC: Cyclin-
(9%–6%): Dizziness, cough, back pain,
dependent kinase inhibitor. CLINI-
hypertension, nausea. CAL: Antineoplastic.

ADVERSE EFFECTS/TOXIC
REACTIONS USES
Upper respiratory tract infection, na-
Used in combination with an aroma-
sopharyngitis, sinusitis, UTI, influenza,
tase inhibitor as initial endocrine-based
bronchitis occur in 5% of pts. Serious in-
therapy for treatment of postmenopausal
fections, including pneumonia, cellulitis,
women with hormone receptor (HR)-
diverticulitis, acute pyelonephritis, occur
positive, human epidermal growth factor
in 3% of pts. Hypersensitivity reaction
receptor 2 (HER2)-negative advanced or
(rash, urticaria, hypotension, dyspnea)
metastatic breast cancer. Used in combi-
occurs rarely. May increase risk of ma-
nation with fulvestrant for treatment of
lignancies.
women with HR-positive, HER2-negative
NURSING CONSIDERATIONS advanced or metastatic breast cancer
with disease progression following en-
BASELINE ASSESSMENT docrine therapy. Used as monotherapy
Assess onset, type, location, duration for treatment of adults with HR-positive,
of pain/inflammation. Inspect appear- HER2-negative advanced or metastatic
ance of affected joint for immobility, breast cancer with disease progression
deformities, skin condition. Screen for following endocrine therapy and prior
latent TB infection prior to initiating chemotherapy in the metastatic setting.
therapy.
PRECAUTIONS
INTERVENTION/EVALUATION Contraindications: Hypersensitivity to
Assess for therapeutic response: relief abemaciclib. Cautions: Baseline anemia,
of pain, stiffness, swelling; increased leukopenia, neutropenia, thrombocyto-
joint mobility; reduced joint tenderness; penia; hepatic/renal impairment, condi-
improved grip strength. Monitor for hy- tions predisposing to infection (e.g., dia-
persensitivity reaction. Diligently screen betes, immunocompromised pts, open
for infection. wounds), history of venous thromboem-
bolism. Avoid concomitant use of strong
PATIENT/FAMILY TEACHING
CYP3A inhibitors, strong CYP3A inducers.
• Notify physician if infection, hyper-
sensitivity reaction, infusion-related re- ACTION
action occurs. • Do not receive live Blocks retinoblastoma tumor suppressor
vaccines during treatment or within 3 protein phosphorylation and prevents
mos of its discontinuation. • COPD pts progression through cell cycle, result-
must report worsening of respiratory ing in arrest of G1 phase. Therapeutic
symptoms. Effect: Inhibits tumor cell growth and
metastasis.
Canadian trade name Non-Crushable Drug High Alert drug
8 abemaciclib
A
PHARMACOKINETICS cracked tablets. • If a dose is missed or
Widely distributed. Metabolized in liver. vomiting occurs, do not give extra dose.
Protein binding: 96.3%. Peak plasma con- Administer next dose at regularly sched-
centration: 8 hrs. Steady-state reached in uled time.
5 days. Excreted in feces (81%), urine
INDICATIONS/ROUTES/
(3%). Half-life: 18.3 hrs.
DOSAGES
LIFESPAN CONSIDERATIONS Breast Cancer
Pregnancy/Lactation: Avoid preg- PO: ADULTS, ELDERLY: Monotherapy:
nancy; may cause fetal harm/malforma- 200 mg twice daily. In combination
tions. Females of reproductive poten- with fulvestrant (and a gonadotro-
tial should use effective contraception pin-releasing hormone agonist if
during treatment and up to 3 wks after pre- or perimenopausal) or an aro-
discontinuation. Unknown if distributed matase inhibitor: 150 mg twice daily.
in breast milk. Breastfeeding not rec- Continue until disease progression or un-
ommended during treatment and up to acceptable toxicity. Recommended dose
3 wks after discontinuation. May impair of fulvestrant is 500 mg once on Days 1,
fertility in males. Children: Safety and 15, 29, then monthly thereafter.
efficacy not established. Elderly: No Dose Reduction for Adverse Events
age-related precautions noted. Monotherapy: Starting dose: 200 mg
INTERACTIONS twice daily. FIRST DOSE REDUCTION: 150
mg twice daily. SECOND DOSE REDUC-
DRUG: Strong CYP3A inhibitors (e.g., TION: 100 mg twice daily. THIRD DOSE
clarithromycin, ketoconazole, ritona- REDUCTION: 50 mg twice daily. In
vir), moderate CYP3A inhibitors (e.g., combination with fulvestrant or
erythromycin, ciprofloxacin, diltia- an aromatase inhibitor: STARTING
zem, dronedarone, fluconazole) may DOSE: 150 mg twice daily. FIRST DOSE
increase concentration/effect. Strong REDUCTION: 100 mg twice daily. SECOND
CYP3A inducers (e.g., carbamazepine, DOSE REDUCTION: 50 mg twice daily.
phenytoin, rifampin) may decrease con-
centration/effect. May decrease effect of Dose Modification
BCG (intravesical), vaccines (live). May Based on Common Terminology Criteria
enhance adverse/toxic effects of natali- for Adverse Events (CTCAE).
zumab, vaccines (live). Pimecrolimus,
tacrolimus may enhance adverse/toxic ef- Diarrhea
fects. HERBAL: Echinacea may decrease Note: At first sign of loose stools, rec-
therapeutic effect. FOOD: Grapefruit ommend treatment with antidiarrheal
products may increase concentration/ agents and hydration.
effect. LAB VALUES: May increase serum Grade 1 diarrhea: No dose adjustment.
ALT, AST, bilirubin, creatinine. May decrease Grade 2 diarrhea: If toxicity does not
ANC, Hgb, Hct, lymphocytes, leukocytes, resolve to Grade 1 or less within 24 hrs,
neutrophils, platelets. withhold treatment until resolved. Then,
resume at same dose level. Recurrent or
AVAILABILITY (Rx) persistent Grade 2 diarrhea at same
Tablets: 50 mg, 100 mg, 150 mg, 200 mg. dose level despite supportive mea-
sures: Withhold treatment until recovery
ADMINISTRATION/HANDLING to Grade 1 or less, then resume at re-
PO duced dose level. Grade 3 or 4 diarrhea
• Give without regard to food. • Ad- or required hospitalization: Withhold
minister whole; do not crush, cut or di- treatment until recovery to Grade 1 or
vide tablets. Do not give broken or less, then resume at reduced dose level.

underlined – top prescribed drug


abemaciclib 9
A
Hematologic Toxicity Dosage in Renal Impairment
Grade 1 or 2 hematologic toxic- Mild to moderate impairment: No
ity: No dose adjustment. Grade 3 he- dose adjustment. Severe impairment,
matologic toxicity: Withhold treat- ESRD: Not specified.
ment until recovery to Grade 2 or less,
then resume at same dose level. Grade 3 Dosage in Hepatic Impairment
(recurrent) or Grade 4 hematologic Mild to moderate impairment: No
toxicity: Withhold treatment until re- dose adjustment. Severe impairment:
covery to Grade 2 or less, then resume at Reduce dose frequency to once daily.
reduced dose level. SIDE EFFECTS
Hepatotoxicity Note: Side effects may vary if pt treated
Grade 1 or 2 hepatotoxicity without concomitantly with an aromatase inhibitor.
serum bilirubin elevation greater Frequent (90%–35%): Diarrhea, fatigue,
than 2 times ULN: No dose adjustment. asthenia, nausea, decreased appetite,
Recurrent or persistent Grade 2 hepa- abdominal pain, vomiting. Occasional
totoxicity; Grade 3 hepatotoxicity (20%–10%): Headache, cough, constipa-
without serum bilirubin elevation tion, arthralgia, dry mouth, decreased
greater than 2 times ULN: Withhold weight, stomatitis, dysgeusia, alopecia,
treatment until recovery to Grade 1 or less, dizziness, pyrexia, dehydration.
then resume at reduced dose level. Serum
ALT, AST elevation greater than 3 ADVERSE EFFECTS/TOXIC
times ULN with serum bilirubin el- REACTIONS
evation greater 2 than times ULN (in Anemia, leukopenia, neutropenia, throm-
the absence of cholestasis); Grade 4 bocytopenia is an expected response to
hepatotoxicity: Permanently discontinue. therapy. Diarrhea occurred in 81–90% of
pts. Grade 3 diarrhea occurred in 9–20%
Other Toxicities of pts. Diarrhea may increase risk of de-
Any other Grade 1 or 2 toxicities: hydration and infection. Neutropenia
No dose adjustment. Recurrent or per- reported in 37–41% of pts. Grade 3 or
sistent Grade 2 toxicity that does 4 hepatotoxicity occurred in up to 4% of
not resolve to Grade 1 (or baseline) pts. Venous thromboembolism including
within 7 days despite supportive cerebral venous thrombosis, subclavian
measures: Withhold treatment until re- and axillary vein thrombosis, inferior
covery to Grade 1 or less, then resume at vena cava thrombosis, DVT, PE, pelvic
reduced dose level. Any other Grade 3 venous thrombosis reported in 5% of
or 4 toxicities: Withhold treatment until pts taking concomitant aromatase inhibi-
resolved to Grade 1 or less, then resume tor therapy. Infections including upper
at reduced dose level. respiratory infection, UTI, pulmonary
Concomitant Use of Strong CYP3A infection occurred in 39% of pts taking
Inhibitors concomitant aromatase inhibitor therapy.
If strong CYP3A inhibitor cannot be dis-
continued, reduce initial dose to 100 mg NURSING CONSIDERATIONS
twice daily if pt taking 200 mg or 150 mg BASELINE ASSESSMENT
twice daily regimen. If dose was already re-
duced to 100 mg twice daily due to adverse Obtain ANC, CBC, BMP, LFT. Confirm
effects, reduce dose to 50 mg twice daily. If HR-positive, HER2-negative status. Ob-
CYP3A inhibitor is discontinued, increase tain pregnancy test prior to initiation.
dose (after 3–5 half-lives of CYP3A inhibi- Question current breastfeeding status.
tor has elapsed) to the dose used prior to Stress importance of antidiarrheal if diar-
initiating strong CYP3A inhibitor. rhea ­occurs. Question history of hepatic

Canadian trade name Non-Crushable Drug High Alert drug


10 abiraterone
A
i­mpairment, venous thromboembolism. take newly prescribed medications unless
Question usual bowel movement patterns, approved by the prescriber who originally
stool characteristics. Receive full medica- started treatment. • Do not ingest grape-
tion history and screen for interactions. fruit products.
Screen for active infection. Assess hydra-
tion status. Offer emotional support.
abiraterone
INTERVENTION/EVALUATION
Monitor CBC for myelosuppression; LFT a-bir-a-ter-one
for hepatotoxicity q2 wks for first 2 mos, (Yonsa, Zytiga)
then monthly for 2 mos, then as clinically Do not confuse Zytiga with Zetia
indicated. Monitor for hepatotoxicity or ZyrTEC.
(abdominal pain, ascites, confusion, dark-
uCLASSIFICATION
colored urine, jaundice). Monitor daily
pattern of bowel activity, stool consistency. PHARMACOTHERAPEUTIC: Anti-
Ensure compliance of antidiarrheal ther- androgen. CLINICAL: Antineoplastic.
apy if diarrhea occurs. If treatment-related
toxicities occur, consider referral to spe-
cialist. Be alert for serious infection, op- USES
portunistic infection, sepsis. Monitor for Treatment of metastatic castration-resistant
venous thromboembolism (arm/leg pain, prostate cancer in combination with
swelling; chest pain, dyspnea, hypoxia, prednisone or methylprednisolone. Treat-
tachycardia). Ensure adequate hydration, ment of metastatic, high-risk castration-
nutrition. Monitor weight, I&Os. sensitive prostate cancer (in combination
with prednisone).
PATIENT/FAMILY TEACHING
• Treatment may depress your immune PRECAUTIONS
system and reduce your ability to fight infec- Contraindications: Hypersensitivity to abi-
tion. Report symptoms of infection such as raterone. Use in women who are pregnant
body aches, burning with urination, chills, or may become pregnant. Cautions: His-
cough, fatigue, fever. Avoid those with active tory of cardiovascular disease (especially
infection. • Report symptoms of bone HF, recent MI, or ventricular arrhythmia)
marrow depression such as bruising, fa- due to potential for hypertension, hypoka-
tigue, fever, shortness of breath, weight loss; lemia, fluid retention; moderate hepatic
bleeding easily, bloody urine or impairment; adrenal insufficiency. Avoid
stool. • Therapy may cause severe diar- use with strong CYP3A4 inducers.
rhea, which may lead to dehydration and
infection. Drink plenty of fluids. Take an- ACTION
tidiarrheal medication as prescribed at the
Selectively and irreversibly inhibits CYP17,
first sign of loose stools. • Treatment may
an enzyme needed for androgen biosyn-
cause fetal harm; avoid pregnancy. • Fe-
thesis (expressed in testicular, adrenal, or
males of child-bearing potential should use
prostatic tumor tissue). Inhibits formation
effective contraception during treatment
of testosterone precursors DHEA and an-
and for at least 3 wks after last dose. Do not
drostenedione. Therapeutic Effect: Low-
breastfeed. • Report symptoms of DVT
ers serum testosterone to castrate levels.
(swelling, pain, hot feeling in the arms or
legs), lung embolism (difficulty breathing,
PHARMACOKINETICS
chest pain, rapid heart rate); liver problems
(bruising, contusion; amber, dark, orange- Protein binding: 99%. Primarily excreted
colored urine; right upper abdominal pain, in feces. Peak plasma concentration:
yellowing of the skin or eyes). • Do not 2 hrs. Half-life: 12 hrs (up to 19 hrs
with hepatic impairment).
underlined – top prescribed drug
abiraterone 11
A
LIFESPAN CONSIDERATIONS 2 times/day). (Zytiga): 1,000 mg once
Pregnancy/Lactation: Contraindi- daily (with predniSONE 5 mg 2 times/day).
cated in women who are or may become Dosage Modification
pregnant. Children: Safety and efficacy Hepatic Enzymes Greater Than Upper
not established. Elderly: No age-related Limit of Normal (ULN) (During Treatment)
precautions noted.
Lab Values Recommendation
INTERACTIONS ALT, AST eleva- Interrupt treatment
tions greater than and restart at 750
DRUG: May increase concentration/effects 5 × ULN or biliru- mg once ALT, AST
of doxorubicin (conventional), thio- bin greater than 3 less than 2.5 × ULN
ridazine. May decrease concentration/ × ULN with 1,000 or bilirubin less
effect of tamoxifen. CYP3A4 inducers mg than 1.5 × ULN.
(e.g., carbamazepine, ketoconazole, ALT, AST eleva- Interrupt treatment
ritonavir), dabrafenib, enzalutamide, tions greater than and restart at 500
lorlatinib may decrease concentration/ 5 × ULN or biliru- mg once ALT, AST
bin greater than 3 less than 2.5 × ULN
effect. HERBAL: St. John’s wort may × ULN with 750 or bilirubin less
decrease levels/effect. FOOD: Do not give mg than 1.5 × ULN.
with food (no food should be consumed
for at least 2 hrs before or 1 hr after dose). If hepatotoxicity occurs at reduced dose
LAB VALUES: May increase serum ALT, of 500 mg daily, discontinue treatment.
AST, bilirubin, triglycerides. May decrease
Dosage Adjustment for Concomitant
serum potassium, phosphate.
Strong CYP3A4 Inducers
AVAILABILITY (Rx) Increase abiraterone dose to 1,000 mg
twice daily.
Tablets: (Yonsa): 125 mg. (Zytiga):
250 mg, 500 mg. Dosage in Renal Impairment
No dose adjustment.
ADMINISTRATION/HANDLING Dosage in Hepatic Impairment
PO Mild impairment: No dosage adjustment
• (Yonsa): May give without regard to necessary. Moderate impairment: Re-
food. • Do not break, crush, dissolve, duce dose to 250 mg daily. Discontinue if
or divide tablets. Give whole with water. serum ALT, AST greater than 5 times ULN or
(Zytiga): • Give on empty stomach serum bilirubin greater than 3 times ULN.
only (at least 1 hr before or 2 hrs after Severe impairment: Avoid use.
food). • Give with water. • Adminis-
ter whole. Do not break, crush, dissolve, SIDE EFFECTS
or divide tablets. Women who are or may Frequent (30%–26%): Joint swelling/discom-
become pregnant should wear gloves if fort, peripheral edema, muscle spasm, mus-
handling the tablets. culoskeletal pain, hypokalemia. Occasional
(19%–6%): Hot flashes, diarrhea, UTI, cough,
INDICATIONS/ROUTES/DOSAGE hypertension, urinary frequency, nocturia.
b ALERT c Consider increased dosage of Rare (less than 6%): Heartburn, upper respi-
predniSONE during unusual stress or infec- ratory tract infection.
tion. Interrupting predniSONE therapy may
induce adrenocorticoid insufficiency. ADVERSE EFFECTS/
TOXIC REACTIONS
Metastatic Castration-Resistant Prostate Mineralocorticoid excess (severe fluid
Cancer retention, hypokalemia, hypertension)
PO: ADULTS, ELDERLY: (Yonsa): 500 mg may compromise pts with prior cardiovas-
once daily (with methylPREDNISolone 4 mg cular history. Safety not established in pts
Canadian trade name Non-Crushable Drug High Alert drug
12 acalabrutinib
A
with left ventricular ejection fraction less condoms during treatment and for 1 wk
than 50%. Tachycardia, atrial fibrillation, after treatment. • Women who are
supraventricular tachycardia, atrial flut- pregnant or are planning pregnancy may
ter, complete AV block, bradyarrhythmia not touch medication without gloves.
reported in 7% of pts. Chest pain, unstable • Dizziness, palpitations, headache,
angina, HF reported in less than 4% of pts. confusion, muscle weakness, leg swell-
Stress, infection, or interruption of daily ing/discomfort may become more appar-
steroids may cause adrenocortical insuf- ent during periods of unusual stress, in-
ficiency. Hepatotoxicity (serum ALT, AST fection, or interruption of predniSONE
greater than 5 times ULN) reported in 2% therapy. • Blood tests will be per-
of pts. Pts with hepatic impairment are formed routinely. • Report signs of
more likely to develop hepatotoxicity. liver problems (yellowing of skin, bruis-
ing, light-colored stool, right upper
NURSING CONSIDERATIONS quadrant pain), chest pain, palpita-
BASELINE ASSESSMENT tions. • An increase in urinary fre-
quency or nocturia is expected as treat-
Obtain baseline BMP, LFT. Evaluate his­­tory ment becomes therapeutic. • Do not
of HF, myocardial infarction, arrhythmias, chew, crush, dissolve, or divide tablets.
angina pectoris, peripheral edema, hepatic
impairment, adrenal or pituitary abnor-
malities, left ventricular ejection fraction (if acalabrutinib
applicable). Question possibility of preg-
nancy before treatment. Question history a-kal-a-broo-ti-nib
of corticosteroid intolerance if applicable. (Calquence)
INTERVENTION/EVALUATION Do not confuse acalabrutinib
with afatinib, cabozantinib,
Assess for peripheral edema behind me- ibrutinib, or lenvatinib.
dial malleolus (sacral area in bedridden
patients). Monitor BMP, LFT. Monitor for uCLASSIFICATION
mineralocorticoid excess (hypokalemia, PHARMACOTHERAPEUTIC: Bruton
hypertension, fluid retention) at least once tyrosine kinase inhibitor. CLINICAL:
monthly. Assess for cardiac arrhythmia Antineoplastic.
if hypokalemia occurs. Obtain ECG for
palpitations, dyspnea, dizziness. Monitor
for signs and symptoms of adrenocortical USES
insufficiency during predniSONE interrup-
tion, periods of stress, infection. Measure Treatment of adults with mantle cell lym-
serum ALT, AST, alkaline phosphatase, bili- phoma (MCL) who have received at least
rubin every 2 wks for 3 mos, then monthly. one prior therapy.
If hepatotoxicity occurs, dosage modifica- PRECAUTIONS
tion will be necessary. Pts with moderate
Contraindications: Hypersensitivity to
hepatic impairment must have LFT every wk
for first month, then every 2 wks for 2 mos, acalabrutinib. Cautions: Baseline ane-
then monthly. If serum ALT, AST above 5 mia, neutropenia, thrombocytopenia; ac-
times ULN or serum bilirubin above 3 times tive infection, conditions predisposing to
ULN, treatment should be discontinued. infection (e.g., diabetes, renal failure, im-
munocompromised pts, open wounds);
PATIENT/FAMILY TEACHING history of atrial fibrillation, atrial flutter;
• Must be taken on empty stomach (no pts at risk for hemorrhage (e.g., history of
food 2 hrs before and 1 hr after dose). intracranial/GI bleeding, coagulation dis-
• If taken with food, toxic levels may orders, recent trauma; concomitant use
result. • Sexually active men must wear of anticoagulants, antiplatelets, NSAIDS).

underlined – top prescribed drug


acalabrutinib 13
A
ACTION ADMINISTRATION/HANDLING
Inhibits enzymatic activity of Bruton PO
tyrosine kinase (BTK); a signaling mol- • Give without regard to food. • Ad-
ecule that promotes malignant B-cell minister whole with a glass of water; do
proliferation and survival. Therapeutic not break, cut, or open capsule. • If a
Effect: Decreases malignant B-cell pro- dose is missed, may administer dose up
liferation and survival. to 3 hrs after regularly scheduled time. If
more than 3 hrs have elapsed, do not give
PHARMACOKINETICS dose. Administer next dose at regularly
Rapidly absorbed and widely distrib- scheduled time. • Give at least 2 hrs
uted. Metabolized in liver. Protein bind- before aluminum-, magnesium-, or cal-
ing: 97.5%. Peak plasma concentration: cium-containing antacids, H2-receptor
0.75 hrs. Steady-state maintained over antagonists.
12 hrs. Excreted in feces (84%), urine
(12%). Half-life: 0.9 hrs (metabolite: INDICATIONS/ROUTES/DOSAGE
6.9 hrs). Mantle Cell Lymphoma
PO: ADULTS, ELDERLY: 100 mg approxi-
LIFESPAN CONSIDERATIONS mately q12h. Continue until disease pro-
Pregnancy/Lactation: Avoid preg- gression or unacceptable toxicity.
nancy; may cause fetal harm. Unknown if Dose Modification
distributed in breast milk. Breastfeeding Based on Common Terminology Criteria
not recommended during treatment and for Adverse Events (CTCAE).
for at least 2 wks after discontinuation. Grade 3 or 4 nonhematologic tox-
Children: Safety and efficacy not estab- icities; Grade 3 thrombocytopenia
lished. Elderly: No age-related precau- with bleeding; Grade 4 thrombo-
tions noted. cytopenia; Grade 4 neutropenia
lasting longer than 7 days: First
INTERACTIONS and second occurrence: Withhold
DRUG: Strong CYP3A4 inhibitors treatment until recovery to Grade 1 or
(e.g., clarithromycin, ketocon- baseline, then resume at 100 mg twice
azole, ritonavir), moderate CYP3A daily. Third occurrence: Withhold
inhibitors (e.g., erythromycin, cip- treatment until recovery to Grade 1 or
rofloxacin, diltiazem, fluconazole, baseline, then resume at 100 mg once
verapamil) may increase concentra- daily. Fourth occurrence: Perma-
tion/effect. Strong CYP3A4 inducers nently discontinue.
(e.g., rifampin, phenytoin, carbam-
azepine, phenobarbital) may decrease Concomitant Use of Strong CYP3A Inhibitors
concentration/effect. May decrease effect Avoid use. If short-term treatment with
of BCG (intravesical), vaccines (live). CYP3A inhibitor is unavoidable (e.g.,
May enhance adverse/toxic effects of na- anti-infectives for up to 7 days), withhold
talizumab, vaccines (live). Pimecro- acalabrutinib until strong CYP3A inhibi-
limus, tacrolimus may enhance adverse/ tor is discontinued.
toxic effects. HERBAL: Echinacea may Concomitant Use of Moderate CYP3A
decrease concentration/effect. St. John’s Inhibitors
wort may decrease concentration/effect. Decrease frequency to 100 mg once daily.
FOOD: None known. LAB VALUES: May
decrease Hgb, platelets, neutrophils. Concomitant Use of Strong CYP3A Inducers
If strong CYP3A inducer cannot be dis-
AVAILABILITY (Rx) continued, increase acalabrutinib dose to
Capsules: 100 mg. 200 mg twice daily.

Canadian trade name Non-Crushable Drug High Alert drug


14 acalabrutinib
A
Dosage in Renal Impairment
and screen for interactions. Offer emo-
Mild to moderate impairment: No
tional support.
dose adjustment. Severe impairment:
Not specified; use caution. INTERVENTION/EVALUATION

Dosage in Hepatic Impairment


Monitor CBC periodically for cytopenias.
Mild to moderate impairment: No
Closely monitor for HBV reactivation;
dose adjustment. Severe impairment: symptoms of PML. Obtain ECG if chest
Not specified; use caution. pain, dyspnea, palpitations occur. Be
alert for serious infection, opportunistic
SIDE EFFECTS infection, sepsis; non-skin carcinomas.
Frequent (39%–18%): Headache, diar-
Monitor for hemorrhagic events including
rhea, fatigue, myalgia, bruising, nausea, intracranial hemorrhage (altered mental
rash. Occasional (15%–13%): Abdominal status, aphasia, blindness, hemiparesis,
pain, constipation, vomiting. unequal pupils, seizures), GI bleeding
(hematemesis, melena, rectal bleeding),
ADVERSE EFFECTS/TOXIC epistaxis. Assess skin for new lesions,
REACTIONS moles. Ensure adequate hydration.
Anemia, neutropenia, thrombocytopenia
PATIENT/FAMILY TEACHING
is an expected response to therapy. Se-
rious and sometimes fatal hemorrhagic • Treatment may depress your im-
events including intracranial hemorrhage, mune system and reduce your ability to
GI bleeding, epistaxis occurred in 2% of fight infection. Report symptoms of in-
pts. Petechiae, bruising reported in 50% fection such as body aches, burning
of pts. Serious bacterial, viral, fungal with urination, chills, cough, fatigue,
infections occurred in 18% of pts. Infec- fever. Avoid those with active infec-
tions due to hepatitis B virus reactivation tion. • Report symptoms of bone
was reported. New primary malignan- marrow depression such as bruising,
cies including skin cancer (7% of pts), fatigue, fever, shortness of breath,
non-skin carcinomas (11% of pts) have weight loss; bleeding easily, bloody
occurred. Progressive Multifocal Leuko- urine or stool. • Avoid pregnancy.
encephalopathy (PML), an opportunistic Breastfeeding not recommended dur-
viral infection of the brain caused by the ing treatment and for at least 2 wks
JC virus may result in progressive perma- after last dose. • PML, an opportu-
nent disability and death. Atrial fibrilla- nistic viral infection of the brain, may
tion/atrial flutter reported in 3% of pts. cause progressive, permanent disabili-
ties and death. Report symptoms of
NURSING CONSIDERATIONS PML, brain hemorrhage such as confu-
sion, memory loss, paralysis, trouble
BASELINE ASSESSMENT speaking, vision loss, seizures, weak-
Obtain ANC, CBC; PT/INR if on antico- ness • Treatment may cause new can-
agulation; pregnancy test. Screen for ac- cers, heart arrhythmias (chest pain,
tive infection. Question history of atrial dizziness, fainting, palpitations, slow
fibrillation, atrial flutter; intracranial/GI or rapid heart rate, irregular heart
bleeding, coagulation disorders, recent rate), reactivation of HBV. • Immedi-
trauma; previous skin cancers. Conduct ately report bleeding of any kind. • Do
baseline dermatological exam and assess not take newly prescribed medications
skin for open/unhealed wounds, lesions, unless approved by the prescriber who
moles. Question current breastfeeding originally started treatment. • Do not
status. Receive full medication history ingest grapefruit products.

underlined – top prescribed drug


acetaminophen 15
A
USES
acetaminophen PO, rectal: Temporary relief of mild to
a-seet-a-min-oh-fen moderate pain, headache, fever.
(Abenol , Acephen, Apo-Acet- IV: (Additional) Management of mod-
aminophen , Atasol , Feverall, erate to severe pain when combined with
Mapap, Ofirmev, Tempra , Tyle- opioid analgesia.
nol, Tylenol Arthritis Pain, Tylenol
Children’s Meltaways, Tylenol Junior
PRECAUTIONS
Meltaways, Tylenol Extra Strength) Contraindications: Hypersensitivity to
j BLACK BOX ALERT j Potential acetaminophen, severe hepatic impair-
for severe liver injury. Acetami- ment or severe active liver disease.
nophen injection associated with Cautions: Sensitivity to acetaminophen;
acute liver failure. severe renal impairment; alcohol depen-
Do not confuse Acephen with Aciphex, dency, hepatic impairment, or active he-
Feverall with Fiberall, Fioricet with patic disease; chronic malnutrition and
Fiorinal, Percocet with Percodan, Tyle-
nol with atenolol, timolol, Tylenol PM, hypovolemia (Ofirmev); G6PD deficiency
or Tylox, or Vicodin with Hycodan. (hemolysis may occur). Limit dose to less
than 4 g/day.
FIXED-COMBINATION(S)
Tylenol with Codeine: acetamino- ACTION
phen/codeine: 120 mg/12 mg per Analgesic: Activates descending sero-
5 mL. Endocet: acetaminophen/ tonergic inhibitory pathways in CNS.
oxyCODONE: 325 mg/5 mg, 325 Antipyretic: Inhibits hypothalamic heat-
mg/7.5 mg, 325 mg/10 mg. Fiori- regulating center. Therapeutic Ef-
cet: acetaminophen/caffeine/butal- fect: Results in antipyresis. Produces
bital: 325 mg/40 mg/50 mg. Hycet: analgesic effect.
acetaminophen/HYDROcodone:
325 mg/7.5 mg per 15 mL. Norco: PHARMACOKINETICS
acetaminophen/HYDROcodone:
Route Onset Peak Duration
325 mg/5 mg, 325 mg/7.5 mg, 325
mg/10 mg. Percocet: acetaminophen/­ PO Less than 1–3 hrs 4–6 hrs
60 min
oxyCODONE: 325 mg/5 mg. Tylenol
with Codeine: acetaminophen/co- Rapidly, completely absorbed from GI
deine: 300 mg/15 mg, 300 mg/30 mg, tract; rectal absorption variable. Protein
300 mg/60 mg. Ultracet: acetamino- binding: 20%–50%. Widely distributed to
phen/traMADol: 325 mg/37.5 mg. Vi- most body tissues. Metabolized in liver.
codin: acetaminophen/HYDROcodone: Excreted in urine. Removed by hemo-
300 mg/5 mg. Vicodin ES: dialysis. Half-life: 1–4 hrs (increased
acetaminophen/HYDROcodone: in pts with hepatic disease, elderly, neo-
300 mg/7.5 mg. Vicodin HP: nates; decreased in children).
acetaminophen/HYDROcodone: 300
mg/10 mg. Xartemis XR: acetamino- LIFESPAN CONSIDERATIONS
phen/oxyCODONE: 325 mg/7.5 mg. Pregnancy/Lactation: Crosses pla-
Xodol: acetaminophen/HYDROcodone: centa; distributed in breast milk. Routinely
300 mg/5 mg, 300 mg/7.5 mg, used in all stages of pregnancy; appears
300 mg/10 mg. safe for short-term use. Children/El-
uCLASSIFICATION derly: No age-related precautions noted.
PHARMACOTHERAPEUTIC: Central INTERACTIONS
analgesic. CLINICAL: Nonnarcotic
analgesic, antipyretic. DRUG: Alcohol (chronic use), hepato-
toxic medications (e.g., phenytoin),
Canadian trade name Non-Crushable Drug High Alert drug
16 acetaminophen
A
hepatic enzyme inducers (e.g., INDICATIONS/ROUTES/DOSAGE
phenytoin, rifAMPin) may increase Note: Over-the-counter (OTC) use of
risk of hepatotoxicity with prolonged acetaminophen should be limited to
high dose or single toxic dose. Da- 3,000 mg/day.
satinib, probenecid may increase
concentration/effect. HERBAL: None Analgesia and Antipyresis
significant. FOOD: Food may decrease IV: ADULTS, ELDERLY, ADOLESCENTS
rate of absorption. LAB VALUES: May WEIGHING 50 KG OR MORE: 1,000 mg
increase serum ALT, AST, bilirubin; q6h or 650 mg q4h. Maximum single
prothrombin levels (may indicate hepa- dose: 1,000 mg; maximum total
totoxicity). daily dose: 4,000 mg. ADULTS, ADO-
LESCENTS WEIGHING LESS THAN 50 KG: 15
AVAILABILITY (OTC) mg/kg q6h or 12.5 mg/kg q4h. Maxi-
Caplets: 325 mg, 500 mg, 650 mg. mum single dose: 750 mg; maxi-
Capsules: 325 mg, 500 mg. Elixir: 160 mum total daily dose: 75 mg/kg/day
mg/5 mL. Injection, Solution (Ofirmev): (3,750 mg). CHILDREN 2–12 YRS: 15 mg/
1,000 mg/100 mL glass vial. Liq- kg q6h or 12.5 mg/kg q4h. Maximum
uid (Oral): 160 mg/5 mL, 500 mg/5 single dose: 750 mg. Maximum: 75
mL, 500 mg/15 mL. Solution (Oral mg/kg/day, not to exceed 3,750 mg/
Drops): 80 mg/0.8 mL. Suppository: 80 day. INFANTS AND CHILDREN LESS THAN
mg, 120 mg, 325 mg, 650 mg. Suspen- 2 YRS (FEVER ONLY): 7.5–15 mg/kg q6h.
sion: 160 mg/5 mL. Syrup: 160 mg/5 Maximum: 60 mg/kg/day. NEONATES
mL. Tablets: 325 mg, 500 mg. Tablets (FEVER ONLY): (Limited data available)
(Chewable): 80 mg. Tablets (Orally Loading dose: 20 mg/kg. PMA 37 or
Disintegrating): 80 mg, 160 mg. greater than 37 wks: 10 mg/kg/
dose q6h. Maximum: 40 mg/kg/day.
Caplets: (Extended-Release [Tylenol
PMA 33–36 wks: 10 mg/kg/dose q8h.
Arthritis Pain]): 650 mg.
Maximum: 40 mg/kg/day. PMA 28–32
ADMINISTRATION/HANDLING wks: 10 mg/kg/dose q12h. Maxi-
mum: 22.5 mg/kg/day.
IV
PO: ADULTS, ELDERLY, CHILDREN 13 YRS
Reconstitution • Does not require AND OLDER: (Regular Strength) 325–650
further dilution. • Store at room tem- mg q4–6h. Maximum: 3,250 mg/day
perature. • Withdraw doses less than unless directed by health care provider.
1,000 mg. • Place in separate empty, Extra Strength: 1000 mg q6h. Maxi-
sterile container. mum: 3,000 mg/day unless directed
Rate of administration • Infuse over by healthcare provider. Extended-
15 min. Release: 1300 mg q8h. Maximum:
Stability • Once opened or transferred, 3,900 mg/day. CHILDREN 12 YRS AND
stable for 6 hrs at room temperature. YOUNGER: (Weight dosing preferred; if
not available, use age. Doses may be re-
PO peated q4h. Maximum: 5 doses/day.)
• Give without regard to food. • Tab-
lets may be crushed. • Do not crush Age Weight (Kg) Dose
extended-release caplets. • Suspen-
11–12 yrs 32.7–43.2 480 mg
sion: Shake well before use. • Take
9–10 yrs 27.3–32.6 400 mg
with full glass of water. 6–8 yrs 21.8–27.2 320 mg
Rectal 4–5 yrs 16.4–21.7 240 mg
2–3 yrs 10.9–16.3 160 mg
• Moisten suppository with cold water
1–<2 yrs 8.2–10.8 120 mg
before inserting well up into rec- 4–11 mos 5.4–8.1 80 mg
tum. • Do not freeze suppositories. 0–3 mos 2.7–5.3 40 mg

underlined – top prescribed drug


acetylcysteine 17
A
NEONATES:Term: 10–15 mg/kg/dose
q4–6h. Maximum: 75 mg/kg/day. NURSING CONSIDERATIONS
GA 33–37 wks or term less than BASELINE ASSESSMENT
10 days: 10–15 mg/kg/dose q6h. If given for analgesia, assess onset, type,
Maximum: 60 mg/kg/day. GA 28–32 location, duration of pain. Effect of medi-
wks: 10–12 mg/kg/dose q6–8h. Maxi- cation is reduced if full pain response re-
mum: 40 mg/kg/day. curs prior to next dose. Assess for fever.
Rectal: ADULTS, ELDERLY, CHILDREN 12
Assess LFT in pts with chronic usage or
YRS AND OLDER: 325–650 mg q4–6h. history of hepatic impairment, alcohol
Maximum: 4 g/24 hrs. CHILDREN: abuse.
(7–11 YRS): 325 mg q4–6h. Maximum:
1,625 mg/day. (4–6 YRS): 120 mg q4–6h. INTERVENTION/EVALUATION
Maximum: 600 mg/day. (1–3 YRS): 80 mg Assess for clinical improvement and re-
q4–6h. Maximum: 400 mg/day. (6–11 lief of pain, fever. Therapeutic serum
mos): 80 mg q6h. Maximum: 320 mg/ level: 10–30 mcg/mL; toxic serum
day. NEONATES: Term: Initially, 30 mg/ level: greater than 200 mcg/mL. Do not
kg/once, then 20 mg/kg/dose q6–8h. exceed maximum daily recommended
Maximum: 75 mg/kg/day. GA 33–37 dose: 4 g/day.
wks or term less than 10 days: Ini-
PATIENT/FAMILY TEACHING
tially, 30 mg/kg once, then 15 mg/kg/
dose q8h. Maximum: 60 mg/kg/day. • Consult physician for use in children
GA 28–32 wks: 20 mg/kg/dose q12h. younger than 2 yrs, oral use longer than
Maximum: 40 mg/kg/day. 5 days (children) or longer than 10 days
(adults), or fever lasting longer than 3
Dosage in Renal Impairment days. • Severe/recurrent pain or high/
Creatinine Clearance Frequency continuous fever may indicate serious
illness. • Do not take more than 4 g/
Oral
10–50 mL/min q6h
day (3 g/day if using OTC [over-the-
Less than 10 mL/min q8h counter]). Actual OTC dosing recom-
Continuous renal q6h mendations may vary by product and/or
­replacement therapy manufacturer. Many nonprescription
IV combination products contain acetamin-
30 mL/min or less (use cau- ophen. Avoid alcohol.
tion, decrease daily dose,
extend dosing interval)

Dosage in Hepatic Impairment


Use with caution. IV contraindicated with acetylcysteine
severe impairment.
a-seet-il-sis-teen
SIDE EFFECTS (Acetadote, Cetylev, Mucomyst ,
Rare: Hypersensitivity reaction. Parvolex )
Do not confuse acetylcysteine
ADVERSE EFFECTS/TOXIC with acetylcholine, or Mucomyst
REACTIONS with Mucinex.
Early Signs of Acetaminophen Toxicity:
Anorexia, nausea, diaphoresis, fatigue uCLASSIFICATION
within first 12–24 hrs. Later Signs of Tox- PHARMACOTHERAPEUTIC: Respiratory
icity: Vomiting, right upper quadrant ten- inhalant, intratracheal. CLINICAL: Mu-
derness, elevated LFTs within 48–72 hrs colytic, antidote acetylcysteine with ace-
after ingestion. Antidote: Acetylcysteine tylcholine, or Mucomyst with Mucinex.
(see Appendix J for dosage).

Canadian trade name Non-Crushable Drug High Alert drug


18 acetylcysteine
A
USES requiring fluid restriction. Store unopened
Inhalation: Adjunctive treatment for ab- vials at room temperature. Following dilu-
normally viscid mucous secretions present tion in D5W, solution is stable for 24 hrs at
in acute and chronic bronchopulmonary room temperature. Color change of opened
disease and in pulmonary complications vials may occur (does not affect potency).
of cystic fibrosis and surgery, diagnostic Three-Bag Method (as Antidote): Loading,
bronchial studies. Injection, PO: Anti- Second, and Third Doses, Pts Weighing
dote in acute acetaminophen toxicity. 40 kg or Greater
Loading dose: 150 mg/kg in 200 mL of
PRECAUTIONS diluent administered over 60 min.
Second dose: 50 mg/kg in 500 mL of di-
Contraindications: Hypersensitivity to
luent administered over 4 hrs.
acetylcysteine. Cautions: Pts with bron-
Third dose: 100 mg/kg in 1,000 mL of
chial asthma; debilitated pts with severe
diluent administered over 16 hrs.
respiratory insufficiency (increases risk
Pts Greater Than 20 kg but Less Than 40 kg
of anaphylactoid reaction).
Loading dose: 150 mg/kg in 100 mL of
ACTION diluent administered over 60 min.
Second dose: 50 mg/kg in 250 mL of di-
Mucolytic splits linkage of mucoproteins,
luent administered over 4 hrs.
reducing viscosity of pulmonary secretions.
Third dose: 100 mg/kg in 500 mL of dilu-
Acetaminophen toxicity: H ­ epatoprotective
ent administered over 16 hrs.
by restoring hepatic glutathione and en-
Pts Less Than or Equal to 20 kg
hancing nontoxic sulfate conjugation of
Loading dose: 150 mg/kg in 3 mL/kg of
acetaminophen. Therapeutic Effect: Fa-
body weight of diluent administered over
cilitates removal of pulmonary secretions
60 min.
by coughing, postural drainage, mechani-
Second dose: 50 mg/kg in 7 mL/kg of body
cal means. Protects against acetamino-
weight of diluent administered over 4 hrs.
phen overdose-induced hepatotoxicity.
Third dose: 100 mg/kg in 14 mL/kg of body
LIFESPAN CONSIDERATIONS weight of diluent administered over 16 hrs.
Pregnancy/Lactation: Unknown if PO
distributed in breast milk. Children/El- • For treatment of acetaminophen over-
derly: No age-related precautions noted. dose. • Give as 5% solution. • Dilute
20% solution 1:3 with cola, orange juice,
INTERACTIONS other soft drink. • Give within 1 hr of
DRUG: None significant. HERBAL: None preparation.
significant. FOOD: None known. LAB
VALUES: None significant. Inhalation, Nebulization
• 20% solution may be diluted with
AVAILABILITY (Rx) 0.9% NaCl or sterile water; 10% solution
Inhalation Solution: (Mucomyst): 10% may be used undiluted.
(100 mg/mL), 20% (200 mg/mL). Injec-
tion Solution: (Acetadote): 20% (200 mg/ IV COMPATIBILITIES
mL). Tablets, Effervescent: 500 mg, 2.5 g. Cefepime (Maxipime), cefTAZidime
(Fortaz).
ADMINISTRATION/HANDLING
IV INDICATIONS/ROUTES/DOSAGE
Bronchopulmonary Disease
The total dose is 300 mg/kg administered Inhalation, Nebulization
over 21 hrs. Dose preparation is based on pt b ALERT c Bronchodilators should be
weight. Total volume administered should be given 10–15 min before acetylcysteine.
adjusted for pts less than 40 kg and for pts
underlined – top prescribed drug
acetylcysteine 19
A
ADULTS, ELDERLY, CHILDREN: 3–5 mL Occasional: Inhalation: Increased
(20% solution) 3–4 times/day or 6–10 bronchial secretions, throat irritation,
mL (10% solution) 3–4 times/day. nausea, vomiting, rhinorrhea. Rare: In-
Range: 1–10 mL (20% solution) q2–6h halation: Rash. PO: Facial edema,
or 2–20 mL (10% solution) q2–6h. IN- bronchospasm, wheezing, nausea, vom-
FANTS: 1–2 mL (20%) or 2–4 mL iting.
(10%) 3–4 times/day.
Intratracheal: ADULTS, CHILDREN: 1–2 ADVERSE EFFECTS/
mL of 10% or 20% solution instilled into TOXIC REACTIONS
tracheostomy q1–4h. Large doses may produce severe nausea/
vomiting. (Less than 2%): Serious ana-
Acetaminophen Overdose phylactoid reactions including cough,
b ALERT c It is essential to initiate wheezing, stridor, respiratory distress,
treatment as soon as possible after over- bronchospasm, hypotension, and death
dose and, in any case, within 24 hrs of have been known to occur with IV ad-
ingestion. ministration.
PO: (Effervescent Tablets, Oral
Solution 5%): ADULTS, ELDERLY, CHIL-
DREN: Loading dose of 140 mg/kg, fol- NURSING CONSIDERATIONS
lowed in 4 hrs by maintenance dose of BASELINE ASSESSMENT
70 mg/kg q4h for 17 additional doses (or
until acetaminophen assay reveals non- Mucolytic: Assess pretreatment respira-
toxic level). Repeat dose if emesis occurs tions for rate, depth, rhythm. IV anti-
within 1 hr of administration. dote: Obtain baseline LFT, PT/INR and
IV: ADULTS, ELDERLY, CHILDREN: (Con-
drug screen. For use as antidote, obtain
sists of 3 doses. Total Dose: 300 mg/kg.) acetaminophen level to determine need
150 mg/kg infused over 60 min, then for treatment with acetylcysteine.
50 mg/kg infused over 4 hrs, then 100 INTERVENTION/EVALUATION
mg/kg infused over 16 hrs (see Adminis-
tration/Handling for dilution). WEIGHING If bronchospasm occurs, discontinue
MORE THAN 100 KG: (Consists of 3 doses.
treatment, notify physician; broncho-
Total Dose: 30 g.) 15 g over 60 min; 5 g dilator may be added to therapy. Moni-
over 4 hrs; 10 g over 16 hrs. Duration tor rate, depth, rhythm, type of respi-
of administration may vary depending on ration (abdominal, thoracic). Observe
acetaminophen levels and LFTs obtained sputum for color, consistency, amount.
during treatment. Pts who still have IV antidote: Administer within 8 hrs
detectable levels of acetaminophen or of acetaminophen ingestion for maxi-
elevated LFT results continue to benefit mal hepatic protection; ideally, within
from additional acetylcysteine adminis- 4 hrs after immediate-release and 2
tration beyond 24 hrs. hrs after liquid acetaminophen formu-
lations.
Diagnostic Bronchial Studies
Inhalation, Nebulization: ADULTS: 1–2 PATIENT/FAMILY TEACHING
mL of 20% solution or 2–4 mL of 10% so- • Slight, disagreeable sulfuric odor
lution 2–3 times before the procedure. from solution may be noticed during
initial administration but disappears
SIDE EFFECTS quickly. • Adequate hydration is im-
IV: (10%): Nausea, vomiting. (7%– portant part of therapy. • Follow
6%): Acute flushing, erythema. (4%): guidelines for proper coughing and
Pruritus. Frequent: Inhalation: Sticki- deep breathing techniques. • Auscul-
ness on face, transient unpleasant odor. tate lung sounds.

Canadian trade name Non-Crushable Drug High Alert drug


20 acyclovir
A
promised pts with cancer; treatment of ini-
acyclovir tial and prophylaxis of recurrent mucosal
and cutaneous herpes simplex infections
a-sye-klo-veer in immunocompromised pts.
(Apo-Acyclovir , Zovirax)
Topical
Do not confuse acyclovir with Cream: Treatment of recurrent herpes
ganciclovir, Retrovir, or valACY­ labialis (cold sores) in immunocompetent
clovir, or Zovirax with Doribax, pts. Ointment: Management of initial gen-
Valtrex, Zithromax, Zostrix, Zy- ital herpes. Treatment of mucocutaneous
loprim, or Zyvox. HSV in immunocompromised pts.
FIXED-COMBINATION(S) PRECAUTIONS
Lipsovir: acyclovir/hydrocortisone Contraindications: Use in neonates when
(a steroid): 5%/1%. acyclovir is reconstituted with Bacterio-
static Water for Injection containing benzyl
uCLASSIFICATION
alcohol. Hypersensitivity to acyclovir, valA-
PHARMACOTHERAPEUTIC: Synthetic CYclovir. Cautions: Immunocompromised
nucleoside. CLINICAL: Antiviral. acy- pts (thrombocytopenic purpura/hemolytic
clovir with ganciclovir, Retrovir, or uremic syndrome reported); elderly, renal
valACYclovir, or Zovirax with Doribax, impairment, use of other nephrotoxic med-
Valtrex, Zithromax, Zostrix, ications. IV Use: Pts with underlying neuro-
Zyloprim, or Zyvox. logic abnormalities, serious hepatic/elec-
trolyte abnormalities, substantial hypoxia.
USES ACTION
Parenteral Acyclovir is converted to acyclovir tri-
Treatment of initial and prophylaxis of re- phosphate, which competes for viral DNA
current mucosal and cutaneous herpes polymerase, becoming part of DNA chain.
simplex virus (HSV-1 and HSV-2) in immu- Therapeutic Effect: Inhibits DNA syn-
nocompromised pts. Treatment of severe thesis and viral replication. Virustatic.
initial episodes of herpes genitalis in immu-
nocompetent pts. Treatment of herpes sim- PHARMACOKINETICS
plex encephalitis including neonatal herpes 15%–30% absorbed from GI tract. Bio-
simplex virus. Treatment of herpes zoster availability: 10%–20%; minimal absorp-
(shingles) in immunocompromised pts. tion following topical application. Protein
Oral binding: 9%–36%. Widely distributed.
Treatment of initial episodes and prophy- Partially metabolized in liver. Excreted
laxis of recurrent herpes simplex (HSV-2 primarily in urine. Removed by hemodi-
genital herpes). Treatment of chickenpox alysis. Half-life: 2.5 hrs (increased in
(varicella). Acute treatment of herpes renal impairment).
zoster (shingles).
OFF-LABEL: (Parenteral/Oral): Preven- LIFESPAN CONSIDERATIONS
tion of HSV reactivation in HIV-positive Pregnancy/Lactation: Crosses placenta;
pts; hematopoietic stem cell transplant distributed in breast milk. Children: Safety
(HSCT); during periods of neutropenia in and efficacy not established in pts younger
pts with cancer; prevention of VZV reacti- than 2 yrs (younger than 1 yr for IV use).
vation in allogenic HSCT; treatment of dis- Elderly: Age-related renal impairment
seminated HSC or VZV in immunocompro- may require decreased dosage. May expe-
mised pts with cancer; empiric treatment rience more neurologic effects (e.g., agita-
of suspected encephalitis in immunocom- tion, confusion, hallucinations).
underlined – top prescribed drug
acyclovir 21
A
INTERACTIONS Cream • Apply to cover only cold
DRUG: Foscarnet may increase nephro- sores or area with symptoms. • Rub
toxic effect. May increase adverse effects until it disappears.
of tizanidine. May decrease therapeutic
effect of Varicilla virus vaccine, zos- IV INCOMPATIBILITIES
ter vaccine. HERBAL: None significant. Aztreonam (Azactam), diltiaZEM (Cardi-
FOOD: None known. LAB VALUES: May zem), DOBUTamine (Dobutrex), DOPamine
increase serum ALT, AST, BUN, creatinine. (Intropin), levoFLOXacin (Levaquin), me-
ropenem (Merrem IV), ondansetron (Zo-
AVAILABILITY (Rx) fran), piperacillin and tazobactam (Zosyn).
Cream: 5%. Injection, Powder for Reconsti-
tution: 500 mg. Injection, Solution: 50 mg/ IV COMPATIBILITIES
mL. Ointment: 5%. Suspension, Oral: 200 Allopurinol (Alloprim), amikacin
mg/5 mL. Tablets: 400 mg, 800 mg. (Amikin), ampicillin, ceFAZolin (Ancef),
Capsules: 200 mg. cefotaxime (Claforan), cefTAZidime (For-
taz), cefTRIAXone (Rocephin), cimetidine
ADMINISTRATION/HANDLING (Tagamet), clindamycin (Cleocin), diphen-
IV hydrAMINE (Benadryl), famotidine (Pep-
cid), fluconazole (Diflucan), gentamicin,
Reconstitution • Add 10 mL Sterile Wa- heparin, HYDROmorphone (Dilaudid),
ter for Injection to each 500-mg vial (50 imipenem (Primaxin), LORazepam (Ati-
mg/mL). Do not use Bacteriostatic Water van), magnesium sulfate, methylPREDNISo-
for Injection containing benzyl alcohol or lone (SOLU), metoclopramide (Reglan),
parabens (will cause precipitate). • Shake metroNIDAZOLE (Flagyl), morphine, multi-
well until solution is clear. • Further di- vitamins, potassium chloride, propofol (Di-
lute with at least 100 mL D5W or 0.9 NaCl. privan), raNITIdine (Zantac), vancomycin.
Final concentration should be 7 mg/mL or
less. (Concentrations greater than 10 mg/ INDICATIONS/ROUTES/DOSAGE
mL increase risk of phlebitis.)
Genital Herpes (Initial Episode)
Rate of administration • Infuse over
IV: ADULTS, ELDERLY: 5–10 mg/kg q8h
at least 1 hr (nephrotoxicity due to crys-
talluria and renal tubular damage may for 2–7 days. Followed with oral therapy
occur with too-rapid rate). • Maintain to complete at least 10 days of therapy.
PO: ADULTS, ELDERLY, CHILDREN 12 YRS
adequate hydration during infusion and
for 2 hrs following IV administration. AND OLDER: 200 mg q4h 5 times/day for 10
Storage • Store vials at room temper-
days or 400 mg 3 times/day for 7–10 days.
CHILDREN YOUNGER THAN 12 YRS: 40–80
ature. • Solutions of 50 mg/mL stable
for 12 hrs at room temperature; may mg/kg/day in 3–4 divided doses for 5–10
form precipitate if refrigerated. • IV days. Maximum: 1,200 mg/day.
Topical: ADULTS: (Ointment): 0.5 inch
infusion (piggyback) stable for 24 hrs at
room temperature. for 4-inch square surface q3h (6 times/
day) for 7 days.
PO
• May give without regard to food. • Do Genital Herpes (Recurrent)
not crush/break capsules. • Store cap- Intermittent Therapy
sules at room temperature. PO: ADULTS, ELDERLY, CHILDREN 12 YRS
AND OLDER: 200 mg q4h 5 times/day for
Topical 5 days or 400 mg 3 times/day for 5–10
Ointment • Avoid contact with eye. days or 800 mg 2 times/day for 5 days
• Use finger cot/rubber glove to prevent or 800 mg 3 times/day for 2 days. CHIL-
autoinoculation. DREN YOUNGER THAN 12 YRS: 20 mg/kg 3

Canadian trade name Non-Crushable Drug High Alert drug


22 acyclovir
A
times/day for 5 days. Maximum: 400 Usual Neonatal Dosage
mg/dose. HSV (treatment) (IV): 20 mg/kg/dose
Chronic Suppressive Therapy q8–12h for 14–21 days.
PO: ADULTS, ELDERLY, CHILDREN 12 YRS HSV (chronic suppression) (PO): 300
AND OLDER: 400 mg 2 times/day for up mg/m2/dose q8h –(after completing a 14–
to 12 mos. CHILDREN YOUNGER THAN 21 day course of IV therapy) for 6 mos.
12 YRS: 20 mg/kg twice daily. Maxi- Varicella-Zoster (IV): 10–15 mg/kg/
mum: 400 mg/dose. dose q8h for 5–10 days.
Herpes Simplex Mucocutaneous Dosage in Renal Impairment
PO: ADULTS, ELDERLY: 400 mg 5 times/ Dosage and frequency are modified
day for 5–10 days. CHILDREN: 20 mg/kg based on severity of infection and degree
4 times/day for 5–7 days. Maximum: of renal impairment.
800 mg/dose. PO: Normal dose 200 mg q4h, 200
IV: ADULTS, ELDERLY, CHILDREN: 5–10 mg q8h, or 400 mg q12h. Creatinine
mg/kg/dose q8h for 7 days. clearance 10 mL/min and less: 200
Topical: ADULTS: (Ointment): 0.5 mg q12h.
inch for 4-inch square surface q3h (6 PO: Normal dose 800 mg q4h. Creati-
times/day) for 7 days. nine clearance greater than 25 mL/
min: Give usual dose and at normal
Herpes Simplex Encephalitis interval, 800 mg q4h. Creatinine clear-
IV: ADULTS, ELDERLY, CHILDREN 12 YRS ance 10–25 mL/min: 800 mg q8h.
AND OLDER: 10 mg/kg q8h for 14–21 Creatinine clearance less than 10
days. CHILDREN 3 MOS–YOUNGER THAN 12 mL/min: 800 mg q12h.
YRS: 10–15 mg/kg q8h for 14–21 days. IV:
Herpes Zoster (Shingles) Creatinine
IV: ADULTS, CHILDREN 12 YRS AND Clearance Dosage
OLDER: (immunocompromised) 10 mg/ Greater than 50 100% of normal q8h
kg/dose q8h for 7–10 days. CHILDREN mL/min
YOUNGER THAN 12 YRS: (immunocom- 25–50 mL/min 100% of normal q12h
promised) 10 mg/kg/dose q8h for 7–10 10–24 mL/min 100% of normal q24h
Less than 10 mL/ 50% of normal q24h
days. min
PO: ADULTS, ELDERLY, CHILDREN 12 YRS Hemodialysis (HD) 2.5–5 mg/kg q24h
AND OLDER: 800 mg q4h 5 times/day for (give after HD)
7–10 days. Peritoneal dialysis 50% normal dose
(PD) q24h
Herpes Labialis (Cold Sores) Continuous renal 5–10 mg/kg q12–24h
Topical: ADULTS, ELDERLY, CHILDREN 12 replacement (q12h for viral me-
YRS AND OLDER: Apply to affected area therapy (CRRT) ningoencephalitis/
5 times/day for 4 days. Buccal Tablet: 50 VZV infection)
mg as a single dose to upper gum region.
Dosage in Hepatic Impairment
Varicella-Zoster (Chickenpox) Mild to moderate impairment: No
b ALERT c Begin treatment within 24 dose adjustment. Severe impairment:
hrs of onset of rash. Use caution.
PO: ADULTS, ELDERLY, CHILDREN OLDER
THAN 12 YRS AND CHILDREN 2–12 YRS,
SIDE EFFECTS
WEIGHING 40 KG OR MORE: 800 mg 4 Frequent: Parenteral (9%–7%): Phlebitis
times/day for 5 days. CHILDREN 2–12 YRS, or inflammation at IV site, nausea,
WEIGHING LESS THAN 40 KG: 20 mg/kg vomiting. Topical (28%): Burn-
4 times/day for 5 days. Maximum: 800 ing, stinging. Occasional: Parenteral
mg/dose. (3%): Pruritus, rash, urticaria.
underlined – top prescribed drug
adalimumab 23
A
PO (12%–6%): Malaise, nausea. j BLACK BOX ALERT jIncreased
Topical (4%): Pruritus. Rare: PO risk for serious infections. Tuberculo-
(3%–1%): Vomiting, rash, diarrhea, sis, invasive fungal infections, bacte-
rial and viral opportunistic infections
headache. Parenteral (2%–1%): have occurred. Test for tuberculosis
Confusion, hallucinations, seizures, prior to and during treatment. Lym-
tremors. Topical (less than 1%): phoma, other malignancies reported
Rash. in children/adolescents. Hepato-
splenic T-cell lymphoma reported
ADVERSE EFFECTS/ primarily in pts with Crohn’s disease
TOXIC REACTIONS or ulcerative colitis and concomitant
azaTHIOprine or mercaptopurine.
Rapid parenteral administration, exces- Do not confuse Humira with
sively high doses, or fluid and electrolyte HumaLOG or HumuLIN, or
imbalance may produce renal failure. Tox- adalimumab with belimumab or
icity not reported with oral or topical use. ipilimumab.
NURSING CONSIDERATIONS uCLASSIFICATION
BASELINE ASSESSMENT PHARMACOTHERAPEUTIC: Mono-
Question for history of allergies, esp. to clonal antibody. CLINICAL: Antirheu-
acyclovir. Assess herpes simplex lesions matic, disease modifying; GI agent;
before treatment to compare baseline TNF blocking agent.
with treatment effect.
INTERVENTION/EVALUATION USES
Assess IV site for phlebitis (heat, pain, Reduces signs/symptoms, progression of
red streaking over vein). Evaluate cutane- structural damage and improves physi-
ous lesions. Ensure adequate ventilation. cal function in adults with moderate to
Manage chickenpox and disseminated severe RA. May be used alone or in com-
herpes zoster with strict isolation. En- bination with other disease-modifying
courage fluid intake. antirheumatic drugs. First-line treatment
of moderate to severe RA, treatment of
PATIENT/FAMILY TEACHING psoriatic arthritis, treatment of anky-
• Drink adequate fluids. • Do not touch losing spondylitis, to induce/maintain
lesions with bare fingers to prevent spread- remission of moderate to severe active
ing infection to new site. • Continue ther- Crohn’s disease, moderate to severe
apy for full length of treatment. • Space plaque psoriasis in pts 6 yrs of age and
doses evenly. • Use finger cot/rubber older. Reduces signs and symptoms of
glove to apply topical ointment. • Avoid moderate to severe active polyarticular
sexual intercourse during duration of le- juvenile rheumatoid arthritis in pts 2 yrs
sions to prevent infecting partner. • Acy- and older. Treatment of active ulcerative
clovir does not cure herpes infec- colitis in pts unresponsive to immuno-
tions. • Pap smear should be done at suppressants. Treatment of moderate to
least annually due to increased risk of cervi- severe hidradenitis suppurativa. Treat-
cal cancer in women with genital herpes. ment of uveitis (noninfectious intermedi-
ate, posterior and panuveitis) in adults.
PRECAUTIONS
adalimumab Contraindications: Hypersensitivity to
adalimumab. Severe infections (e.g., sep-
a-da-lim-ue-mab sis, TB). Cautions: Pts with chronic in-
(Cyltezo, Humira) fections or pts at risk for infections (e.g.,

Canadian trade name Non-Crushable Drug High Alert drug


24 adalimumab
A
diabetes, indwelling catheters, renal fail- ADMINISTRATION/HANDLING
ure, open wounds), elderly, decreased SQ
left ventricular function, HF, demyelinat- • Refrigerate; do not freeze. • Discard
ing disorders, invasive fungal infections, unused portion. • Rotate injection sites.
history of malignancies. Give new injection at least 1 inch from an
old site and never into area where skin is
ACTION
tender, bruised, red, or hard. • Give in
Binds specifically to tumor necrosis fac- thigh or lower abdomen. • Avoid areas
tor (TNF) alpha cell, blocking its interac- within 2 inches of navel.
tion with cell surface TNF receptors and
cytokine-driven inflammatory processes. INDICATIONS/ROUTES/DOSAGE
Therapeutic Effect: Decreases signs/ Rheumatoid Arthritis (RA)
symptoms of RA, psoriatic arthritis, ankylos- SQ: ADULTS, ELDERLY: 40 mg every
ing spondylitis, Crohn’s disease, ulcerative other wk. Dose may be increased to 40
colitis. Inhibits progression of rheumatoid mg/wk in pts not taking methotrexate.
and psoriatic arthritis. Reduces epidermal
thickness, inflammation of plaque psoriasis. Ankylosing Spondylitis, Psoriatic Arthritis
SQ: ADULTS, ELDERLY: 40 mg every
PHARMACOKINETICS other wk.
Metabolism not specified. Elimination Crohn’s Disease
not specified. Half-life: 10–20 days. SQ: ADULTS, ELDERLY, CHILDREN 6 YRS
AND OLDER WEIGHING 40 KG OR MORE: Ini-
LIFESPAN CONSIDERATIONS tially, 160 mg given as 4 injections on
Pregnancy/Lactation: Unknown if dis- day 1 or 2 injections/day over 2 days,
tributed in breast milk. Children: Safety then 80 mg 2 wks later (day 15). Main-
and efficacy not established. Elderly: Cau- tenance: 40 mg every other wk begin-
tious use due to increased risk of serious ning at day 29. CHILDREN 6 YRS AND OLDER
infection and malignancy. WEIGHING 17–39 KG: 80 mg (2 40-mg
injections on day 1), then 40 mg 2 wks
INTERACTIONS later. Maintenance: 20 mg every other
DRUG: May increase the adverse effects wk beginning at day 29.
of abatacept, anakinra, belimumab, Plaque Psoriasis, Uveitis
canakinumab, natalizumab, tofaci- SQ: ADULTS, ELDERLY: Initially, 80 mg as
tinib, vaccines (live), vedolizumab. a single dose, then 40 mg every other wk
May decrease the therapeutic effect of starting 1 wk after initial dose.
BCG (intravesical), vaccines (live).
May increase the immunosuppressive Juvenile Rheumatoid Arthritis
effects of certolizumab, infliximab. SQ: CHILDREN 2 YRS AND OLDER, WEIGH-
Tocilizumab may increase immuno- ING 10–14 KG: 10 mg ­ every other wk.
suppressive effect. HERBAL: Echina- WEIGHING 15–29 KG: 20 mg every other
cea may decrease effects. FOOD: None wk. WEIGHING 30 KG OR MORE: 40 mg ev-
known. LAB VALUES: May increase se- ery other wk.
rum cholesterol, other lipids, alkaline
phosphatase. Ulcerative Colitis
SQ: ADULTS, ELDERLY: Initially, 160 mg
AVAILABILITY (Rx) (4 injections in 1 day or 2 injections over
2 consecutive days) then 80 mg 2 wks
Injection Solution: 10 mg/0.2 mL, 10 later (day 15), then 40 mg every other
mg/0.1 mL, 20 mg/0.2 mL, 20 mg/0.4 mL, wk beginning on day 29.
40 mg/0.8 mL, 40 mg/0.4 mL, 80 mg/0.8
mL in prefilled syringes.
underlined – top prescribed drug
adefovir 25
A
Hidradenitis Suppurativa
PATIENT/FAMILY TEACHING
SQ: ADULTS, ELDERLY: Initially, 160 mg
(4 injections day 1) or 80 mg (2 injec- • Injection site reaction generally oc-
tions on days 1 and 2), then 80 mg 2 wks curs in first month of treatment and de-
later (day 15), then 40 mg weekly begin- creases in frequency during continued
ning day 29. therapy. • Do not receive live vaccines
during treatment. • Report rash, nau-
Dosage in Renal/Hepatic Impairment sea. • A healthcare provider will show
No dose adjustment. you how to properly prepare and inject
your medication. You must demonstrate
SIDE EFFECTS correct preparation and injection tech-
Frequent (20%): Injection site erythema, niques before using medication.
pruritus, pain, swelling. Occasional
(12%–9%): Headache, rash, sinusitis,
nausea. Rare (7%–5%): Abdominal or adefovir
back pain, hypertension.
a-def-o-veer
ADVERSE EFFECTS/ (Hepsera)
TOXIC REACTIONS j BLACK BOX ALERT jMay cause
Hypersensitivity reactions (rash, urticaria, HIV resistance in unrecognized or
hypotension, dyspnea), infections (pri- untreated HIV infection. Lactic acido-
marily upper respiratory tract, bronchitis, sis, severe hepatomegaly with stea-
tosis (fatty liver), acute exacerbation
urinary tract) occur rarely. May increase of hepatitis have occurred. Use with
risk of serious infections (pneumonia, tu- caution in pts with renal dysfunction
berculosis, cellulitis, pyelonephritis, septic or in pts at risk for renal toxicity.
arthritis). May increase risk of reactivation
of hepatitis B virus in pts who are chronic uCLASSIFICATION
carriers. May cause new-onset or exacer- PHARMACOTHERAPEUTIC: Reverse
bation of central nervous demyelinating transcriptor inhibitor, nucleotide (an-
disease; worsening and new-onset HF. May ti-HBV). CLINICAL: Antihepadnaviral.
increase risk of malignancies. Immunoge-
nicity (anti-adalimumab autoantibodies)
occured in 12% of pts. USES
Treatment of chronic hepatitis B virus
NURSING CONSIDERATIONS infection in adults with evidence of ac-
BASELINE ASSESSMENT tive viral replication based on persistent
elevations of serum ALT or AST or histo-
Assess onset, type, location, duration of logic evidence.
pain or inflammation. Inspect appear-
ance of affected joints for immobility, PRECAUTIONS
deformities, skin condition. Review im- Contraindications: Hypersensitivity to
munization status/screening for TB. If pt adefovir. Cautions: Pts with known risk
is to self-administer, instruct on SQ injec- factors for hepatic disease (female gen-
tion technique, including areas of the der, obesity, prolonged treatment), renal
body acceptable for injection sites. impairment, elderly. Concurrent adminis-
INTERVENTION/EVALUATION tration with tenofovir-containing products.
Monitor lab values, particularly CBC. As- ACTION
sess for therapeutic response: relief of
pain, stiffness, swelling; increased joint Interferes with hepatitis B viral RNA-de-
mobility; reduced joint tenderness; im- pendent DNA polymerase. Therapeutic
proved grip strength. Effect: Inhibits viral replication.

Canadian trade name Non-Crushable Drug High Alert drug


26 adenosine
A
PHARMACOKINETICS SIDE EFFECTS
Rapidly converted to adefovir in intestine. Frequent (13%): Asthenia. Occasional
Binds to proteins after PO administration. (9%–4%): Headache, abdominal pain,
Protein binding: less than 4%. Excreted nausea, flatulence. Rare (3%): Diarrhea,
in urine. Half-life: 7 hrs (increased in dyspepsia.
renal impairment).
ADVERSE EFFECTS/
LIFESPAN CONSIDERATIONS TOXIC REACTIONS
Pregnancy/Lactation: Unknown if Nephrotoxicity, characterized by in-
drug crosses placenta or is distributed creased serum creatinine and decreased
in breast milk. Children: Safety and glomerular filtration rate (GFR), is treat-
efficacy not established. Elderly: Age- ment-limiting toxicity of adefovir therapy.
related renal impairment, decreased car- Lactic acidosis, severe hepatomegaly oc-
diac function require cautious use. cur rarely, particularly in female pts.

INTERACTIONS NURSING CONSIDERATIONS


DRUG: May alter effects of tenofovir BASELINE ASSESSMENT
(avoid concomitant use). HERBAL: None Obtain baseline renal function lab values
significant. FOOD: Alcohol may increase before therapy begins and routinely there-
risk of hepatotoxicity. LAB VALUES: May after. Pts with renal insufficiency, preexist-
increase serum ALT, AST, amylase. ing or during treatment, may require dose
adjustment. HIV antibody testing should
AVAILABILITY (Rx) be performed before therapy begins (un-
Tablets: 10 mg. recognized or untreated HIV infection may
result in emergence of HIV resistance).
ADMINISTRATION/HANDLING
INTERVENTION/EVALUATION
PO
• Give without regard to food. Monitor I&O. Closely monitor for adverse
reactions in those taking other medica-
INDICATIONS/ROUTES/DOSAGE tions that are excreted renally or with
other drugs known to affect renal function.
Note: Continue for 6 months or longer
after HBeAg seroconversion. PATIENT/FAMILY TEACHING

Chronic Hepatitis B (Normal Renal


• Report nausea, vomiting, abdominal
Function)
pain. • Avoid alcohol. • Do not take
PO: ADULTS, ELDERLY, CHILDREN 12 YRS
over-the-counter anti-inflammatory
AND OLDER: 10 mg once daily. drugs. • Report decreased urinary out-
put, dark-colored urine.
Chronic Hepatitis B (Impaired Renal
Function)
PO: ADULTS, ELDERLY WITH CREATI-
NINE CLEARANCE 20–49 ML/MIN: 10 mg
adenosine
q48h. ADULTS, ELDERLY WITH CREATI- ah-den-oh-seen
NINE CLEARANCE 10–19 ML/MIN: 10 mg
(Adenocard)
q72h. ADULTS, ELDERLY ON HEMODI-
ALYSIS: 10 mg every 7 days following uCLASSIFICATION
dialysis. PHARMACOTHERAPEUTIC: Cardiac
Dosage in Hepatic Impairment agent, diagnostic aid. CLINICAL: An-
No adjustment needed. tiarrhythmic.

underlined – top prescribed drug


adenosine 27
A
USES HERBAL: None significant. FOOD: Avoid
Adenocard: Treatment of paroxysmal su- caffeine (may decrease effect). LAB
praventricular tachycardia (PSVT), includ- VALUES: None significant.
ing pts associated with accessory bypass
AVAILABILITY (Rx)
tracts (Wolff-Parkinson-White syndrome).
Adjunct in diagnosis in myocardial perfu- Injection Solution: (Adenocard): 3 mg/
sion imaging or stress echocardiography. mL in 2-mL, 4-mL, 20-mL, 30-mL vials.
OFF-LABEL: Acute vasodilator testing in pul-
ADMINISTRATION/HANDLING
monary artery hypertension.
IV
PRECAUTIONS Rate of administration • Administer
Contraindications: Hypersensitivity to ad- very rapidly (over 1–2 sec) undiluted di-
enosine. Second- or third-degree AV block, rectly into vein, or if using IV line, use
symptomatic bradycardia (except in pts closest port to insertion site. If IV line is
with functioning pacemaker), sick sinus infusing any fluid other than 0.9% NaCl,
syndrome. Bronchoconstrictive or broncho- flush line first. • After rapid bolus injec-
spastic lung disease, asthma. Cautions: Pts tion, follow with 0.9% NaCl rapid flush, B/P.
with first-degree AV block, bundle branch Storage • Store at room temperature.
block; concurrent use of drugs that slow AV Solution appears clear. • Crystallization
conduction (e.g., digoxin, verapamil); auto- occurs if refrigerated; if crystallization oc-
nomic dysfunction, pericarditis, pleural effu- curs, dissolve crystals by warming to room
sion, carotid stenosis, uncorrected hypovo- temperature. • Discard unused portion.
lemia; elderly, pts with bronchoconstriction.
IV INCOMPATIBILITIES
ACTION Any drug or solution other than 0.9% NaCl,
Antiarrhythmic: Slows impulse formation D5W, Ringer’s lactate, or abciximab.
in SA node and conduction time through
AV node. Interrupts the reentry pathways INDICATIONS/ROUTES/DOSAGE
through A-V node. Acts as a diagnostic aid in Paroxysmal Supraventricular Tachycardia
myocardial perfusion imaging or stress echo- (PSVT) (Adenocard)
cardiography by causing coronary vasodila- Rapid IV bolus: ADULTS, ELDERLY, CHIL-
tion and increased blood flow. Therapeutic DREN WEIGHING 50 KG OR MORE: Initially, 6
Effect: Restores normal sinus rhythm. mg given over 1–2 sec. If first dose does
not convert within 1–2 min, give 12 mg;
PHARMACOKINETICS may repeat 12-mg dose in 1–2 min if no
Rapidly cleared from circulation via cellular response has occurred. Follow each dose
uptake. Metabolized via phosphorylation or with 20 mL 0.9% NaCl by rapid IV push.
deamination. Half-life: Less than 10 secs. CHILDREN WEIGHING LESS THAN 50 KG: Ini-
tially 0.05–0.1 mg/kg. (Maximum: 6
LIFESPAN CONSIDERATIONS mg). If first dose does not convert within
Pregnancy/Lactation: Unknown if dis- 1–2 min, may increase dose by 0.05–0.1
tributed in breast milk. Do not breastfeed mg/kg. May repeat until sinus rhythm is es-
until approved by physician. Children/El- tablished or up to a maximum single dose
derly: No age-related precautions noted. of 0.3 mg/kg or 12 mg. Follow each dose
with 5–10 mL 0.9% NaCl by rapid IV push.
INTERACTIONS
DRUG: Methylxanthines (e.g., the- Diagnostic Testing (Adenoscan)
ophylline) may decrease effect. Dipyri- IV infusion: ADULTS: 140 mcg/kg/min
damole, nicotine may increase effect. for 6 min using syringe or infusion pump.
CarBAMazepine may increase degree Total dose: 840 mcg/kg. Thallium is in-
of heart block caused by adenosine. jected at midpoint (3 min) of infusion.
Canadian trade name Non-Crushable Drug High Alert drug
28 ado-trastuzumab emtansine
A
Dosage in Renal/Hepatic Impairment uCLASSIFICATION
No dose adjustment. PHARMACOTHERAPEUTIC: Anti-
HER2. Antibody drug conjugate. Anti-
SIDE EFFECTS microtubular. Monoclonal antibody.
Frequent (18%–12%): Facial flushing, CLINICAL: Antineoplastic.
dyspnea. Occasional (7%–2%): Head-
ache, nausea, light-headedness, chest
pressure. Rare (1% or less): Paresthesia, USES
dizziness, diaphoresis, hypotension, pal- Treatment of HER2-positive, metastatic
pitations; chest, jaw, or neck pain. breast cancer in pts who have previ-
ously received trastuzumab and a tax-
ADVERSE EFFECTS/ ane agent separately or in combination,
TOXIC REACTIONS or pts who have developed recurrence
Frequently produces transient, short- within 6 mos of completing adjuvant
lasting heart block. therapy. Treatment (single agent) of hu-
man epidermal growth factor receptor
NURSING CONSIDERATIONS 2 (HER2)–positive early breast cancer
BASELINE ASSESSMENT in pts with residual invasive disease af-
ter taxane and trastuzumab-based treat-
Identify arrhythmia per cardiac monitor, ment.
12-lead ECG, and assess apical pulse, B/P.
INTERVENTION/EVALUATION PRECAUTIONS
Assess cardiac performance per continu- Contraindications: Hypersensitivity to
ous ECG. Monitor B/P, apical pulse (rate, trastuzumab. Cautions: History of cardio-
rhythm, quality). Monitor respiratory myopathy, HF, MI, arrhythmias, hepatic
rate. Monitor serum electrolytes. disease, thrombocytopenia, pulmonary
disease, peripheral neuropathy, pregnancy.
PATIENT/FAMILY TEACHING
• May induce feelings of impending ACTION
doom, which resolves quickly. • Flush- Binds to HER2 receptor and undergoes
ing/headache may occur temporarily receptor-mediated lysosomal degradation,
following administration. • Report con­ resulting in intracellular release of DM1-
tinued chest pain, light-headedness, head containing cytotoxic catabolites. Binding
or neck pain, difficulty breathing. of DM1 to tubulin disrupts microtubule
networks in the cell. Therapeutic Ef-
fect: Inhibits tumor cell survival in HER2-
ado-trastuzumab positive breast cancer.

emtansine PHARMACOKINETICS
Metabolized in liver. Protein binding:
ado-tras-tooz-oo-mab 93%. Peak plasma concentration: 30–90
(Kadcyla) min. Half-life: 4 days.
j BLACK BOX ALERT j Do not LIFESPAN CONSIDERATIONS
substitute ado-trastuzumab for trastu-
zumab. Hepatotoxicity, hepatic failure Pregnancy/Lactation: May cause fetal
may lead to death. Monitor hepatic harm. Use contraception during treatment
function prior to each dose. May de- and up to 6 mos after discontinuation. Un-
crease left ventricular ejection fraction known if distributed in breast milk. Do not
(LVEF). Embryo-fetal toxicity may result
in birth defects and/or fetal demise. breastfeed. Children: Safety and efficacy
Do not confuse ado-trastuzum- not established. Elderly: No age-related
ab with trastuzumab. precautions noted.

underlined – top prescribed drug


ado-trastuzumab emtansine 29
A
INTERACTIONS Metastatic Breast Cancer
DRUG: May decrease the therapeutic effect IV infusion: ADULTS/ELDERLY: 3.6 mg/
of BCG (intravesical), vaccines (live). kg every 3 wks until disease progression
May increase adverse effects of belimumab, or unacceptable toxicity.
natalizumab, vaccines (live). Strong
Breast Cancer, Early, HER2 Positive,
CYP3A4 inhibitors (e.g., clarithromy-
Adjuvant Therapy
cin, ketoconazole, ritonavir) may in-
IV infusion: ADULTS/ELDERLY: 3.6 mg/kg
crease concentration/effect. HERBAL: Echi-
q3wks for 14 cycles (in the absence of dis-
nacea may decrease therapeutic effect.
ease recurrence or unacceptable toxicity).
FOOD: None known. LAB VALUES: May
Maximum: 3.6 mg/kg.
increase serum ALT, AST, bilirubin. May de-
crease platelets, serum potassium. Dose Modification
Reduction Schedule for Adverse Effects
AVAILABILITY (Rx)
Initial dose: 3.6 mg/kg. First reduction:
Lyophilized Powder for Injection: 100-mg 3 mg/kg. Second reduction: 2.4 mg/kg.
vial, 160-mg vial. Elevated serum ALT, AST: If less than
ADMINISTRATION/HANDLING 5 times upper limit of normal (ULN), con-
tinue same dose. If 5–20 times ULN, hold
b ALERT c Use 0.22-micron in-line fil- until less than 5 times ULN and reduce by
ter. Do not administer IV push or bolus. one dose level. If greater than 20 times
IV ULN, discontinue. Elevated serum bili-
rubin: Hold until less than 1.5 times ULN,
Reconstitution • Use proper chemo- then continue same dose. If 3–10 times
therapy precautions. • Slowly inject 5 mL ULN, hold until less than 1.5 times ULN,
of Sterile Water for Injection into 100-mg then reduce by one dose level. If greater
vial or 8 mL Sterile Water for Injection for than 10 times ULN, discontinue. Left ven-
160-mg vial. • Final concentration: 20 tricular dysfunction: If LVEF greater
mg/mL. • Gently swirl until completely than 45%, continue same dose. If LVEF
dissolved. • Do not shake. • Inspect for 40%–45% with a decrease less than 10%
particulate matter/discoloration. • Calcu- from baseline, continue dose (or reduce)
late dose from 20 mg/mL vial. • Further and repeat LVEF in 3 wks. If LVEF 40%–45%
dilute in 250 mL of 0.9% NaCl only. • In- with decrease greater than 10% from base-
vert bag to mix (do not shake). line, hold and repeat assessment in 3 wks.
Rate of administration • Infuse us- Discontinue therapy if no recovery within
ing 0.22-micron in-line filter. • Infuse 10% of baseline, LVEF less than 40%, or
initial dose over 90 min. • Infuse sub- symptomatic HF. Thrombocytopenia: If
sequent doses over 30 min. • Slow or platelet count is 25,000–50,000 cells/mm3,
interrupt infusion rate if hypersensitivity hold until level greater than 75,000 cells/
reaction occurs. mm3 and then continue same dose. If plate-
Storage • Refrigerate unused vi- let count is less than 25,000 cells/mm3,
als. • Reconstituted vials, diluted solu- hold until level greater than 75,000 cells/
tions should be used immediately (may mm3 and reduce one dose level.
be refrigerated for up to 24 hrs).
Dosage in Renal/Hepatic Impairment
IV INCOMPATIBILITIES No dose adjustment.
Do not use dextrose-containing solutions.
SIDE EFFECTS
INDICATIONS/ROUTES/DOSAGE Frequent (40%–21%): Nausea, fatigue, mus-
Note: Do not substitute with conven- culoskeletal pain, headache, constipation,
tional trastuzumab (Herceptin). diarrhea. Occasional (19%–7%): ­Abdominal

Canadian trade name Non-Crushable Drug High Alert drug


30 afatinib
A
pain, vomiting, pyrexia, arthralgia, asthe- up to 6 mos after discontinuation. • Re-
nia, cough, dry mouth, stomatitis, myalgia, port black/tarry stools, RUQ abdominal
insomnia, rash, dizziness, dyspepsia, pain, nausea, bruising, yellowing of skin or
chills, dysgeusia, peripheral edema. eyes, difficulty breathing, palpitations,
Rare (6%–3%): Pruritus, blurry vision, bleeding. • Avoid alcohol. • Treatment
dry eye, conjunctivitis, lacrimation. may reduce the heart’s ability to pump;
expect routine echocardiograms. • Re-
ADVERSE EFFECTS/ port bleeding of any kind or extremity
TOXIC REACTIONS numbness, tingling, weakness, pain.
Hepatotoxicity may include elevated trans-
aminase, nodular regenerative hyperpla-
sia, portal hypertension. Left ventricular
dysfunction reported in 1.8% of pts.
afatinib
Interstitial lung disease (ILD), including a-fa-ti-nib
pneumonitis, may lead to ARDS. Hyper- (Gilotrif)
sensitivity reactions reported in 1.4% of Do not confuse afatinib with
pts. Thrombocytopenia (34% of pts) may ibrutinib, dasatinib, gefitinib,
increase risk of bleeding. Peripheral neu- or SUNItinib.
ropathy observed rarely. Approx. 5.3%
of pts tested positive for anti–ado-trastu- uCLASSIFICATION
zumab antibodies (immunogenicity). PHARMACOTHERAPEUTIC: Epidermal
NURSING CONSIDERATIONS growth factor receptor (EGFR) inhibi-
tor. Tyrosine kinase inhibitor. CLINI-
BASELINE ASSESSMENT CAL: Antineoplastic.
Obtain baseline CBC, BMP; PT/INR if on
anticoagulants. Confirm HER2-positive titer.
Screen for baseline HF, hepatic impairment, USES
peripheral edema, pulmonary disease, First-line treatment of metastatic non–
thrombocytopenia. Obtain negative preg- small-cell lung cancer (NSCLC) in pts
nancy test before initiating treatment. Ques- with epidermal growth factor (EDGF)
tion current breastfeeding status. Obtain exon 19 deletions or exon 21 (L858R)
baseline echocardiogram for LVEF status. substitution mutations. Treatment of
metastatic, squamous NSCLC progressing
INTERVENTION/EVALUATION after platinum-based chemotherapy.
Observe for hypersensitivity reactions
during infusion. Monitor LFT, potassium PRECAUTIONS
levels before and during treatment. Obtain Contraindications: Hypersensitivity to
LVEF q3mos or with any dose reduction afa­tinib. Cautions: Hepatic impairment;
regarding LVEF status. Assess for bruis- severe renal impairment; pts with hx of
ing, jaundice, right upper quadrant (RUQ) keratitis, severe dry eye, ulcerative kerati-
abdominal pain. Obtain anti–ado-trastu- tis, or use of contact lenses; hypovolemia;
zumab antibody titer if immunogenicity pulmonary disease; ulcerative lesions.
suspected. Obtain stat ECG for palpitations Patients with GI disorders associated with
or irregular pulse, chest X-ray for difficulty diarrhea (e.g., Crohn’s disease), cardiac
breathing, cough, fever. Monitor for neu- risk factors, and/or decreased left ven-
rotoxicity (peripheral neuropathy). tricular ejection fraction.
PATIENT/FAMILY TEACHING ACTION
• Blood levels will be monitored rou- Highly selective blocker of ErbB family
tinely. • Avoid pregnancy. • Contracep- (e.g., EGFR, HER2); irreversibly binds
tion should be used during treatment and
underlined – top prescribed drug
afatinib 31
A
to intracellular tyrosine kinase domain. Dose Modification
Therapeutic Effect: Inhibits tumor Chronic use of P-glycoprotein (P-gp)
growth, causes tumor regression. inhibitors: Reduce daily dose by 10 mg.
Resume previous dose after discontinuation
PHARMACOKINETICS of inhibitor if tolerated. Chronic use of P-
Readily absorbed following PO ad- glycoprotein inducers: Increase daily
ministration. Enzymatic metabolism is dose by 10 mg if tolerated. May resume
minimal. Protein binding: 95%. Peak initial dose 2–3 days after discontinuation
plasma concentration: 2–5 hrs. Ex- of P-gp inducer. Moderate to severe
creted in feces (85%), urine (4%). diarrhea (more than 48 hrs): With-
Half-life: 37 hrs. hold dose until resolution to mild diarrhea.
Moderate cutaneous skin reaction
LIFESPAN CONSIDERATIONS (more than 7 days): Withhold dose until
Pregnancy/Lactation: May cause fetal reaction resolves, then reduce dose appro-
harm. Unknown if distributed in breast priately. Suspected keratitis: Withhold
milk. Must either discontinue drug or dis- until appropriately ruled out. If keratitis
continue breastfeeding. Contraception rec- confirmed, continue only if benefits out-
ommended during treatment and up to 2 weigh risks.
wks after discontinuation. Children: Safety Permanent Discontinuation
and efficacy not established. Elderly: No Discontinue if persistent severe diarrhea,
age-related precautions noted. respiratory distress, severe dry eye, or
INTERACTIONS life-threatening bullous, blistering, exfo-
liating lesions, persistent ulcerative kera-
DRUG: P-glycoprotein inhibitors (e.g., titis, interstitial lung disease, symptom-
amiodarone, cycloSPORINE, keto- atic left ventricular dysfunction occurs.
conazole) may increase concentra-
tion/effect. P-glycoprotein inducers Dosage in Renal/Hepatic Impairment
(e.g., carBAMazepine, rifAMPin) eGFR 15–29 mL/min: Decrease dose to
may decrease concentration/effect. 30 mg. Severe impairment: Avoid use.
HERBAL: None significant. FOOD: High-
fat meals may decrease absorption. LAB SIDE EFFECTS
VALUES: May increase serum ALT, AST. Frequent (96%–58%): Diarrhea, rash,
May decrease serum potassium. dermatitis, stomatitis, paronychia (nail
infection). Occasional (31%–11%): Dry
AVAILABILITY (Rx) skin, decreased appetite, pruritus,
Tablets: 20 mg, 30 mg, 40 mg. epistaxis, weight loss, cystitis, pyrexia,
cheilitis (lip inflammation), rhinorrhea,
ADMINISTRATION/HANDLING conjunctivitis.
PO
• Give at least 1 hr before or 2 hrs after ADVERSE EFFECTS/TOXIC
meal. Do not take missed dose within 12 REACTIONS
hrs of next dose. Diarrhea may lead to severe, sometimes
fatal, dehydration or renal impairment.
INDICATIONS/ROUTES/DOSAGE Bullous and exfoliative skin lesions oc-
Metastatic NSCLC, Metastatic Squamous cur rarely. Rash, erythema, acneiform
NSCLC lesions occur in 90% of pts. Palmar-
PO: ADULTS/ELDERLY: Initially, 40 mg plantar erythrodysesthesia syndrome
once daily until disease progression or (PPES), a chemotherapy-induced skin
no longer tolerated. Do not take missed condition that presents with redness,
dose within 12 hrs of next dose. swelling, numbness, skin sloughing of

Canadian trade name Non-Crushable Drug High Alert drug


32 albumin
A
the hands and feet, has been reported.
Interstitial lung disease (ILD), includ- albumin
ing pulmonary infiltration, pneumonitis,
ARDS, allergic alveolitis, reported in 2% al-bue-min
of pts. Hepatotoxicity reported in 10% (Albuked-5, Albuked-25,
of pts. Keratitis symptoms, such as eye Albuminar-5, Albuminar-25,
inflammation, lacrimation, light sensi- AlbuRx, Albutein, Buminate,
tivity, blurred vision, red eye, occurred Flexbumin, ­Kedbumin, Plasbumin-5,
in 1% of pts. ­Plasbumin-25)
Do not confuse albumin with
NURSING CONSIDERATIONS albuterol, or Buminate with
bumetanide.
BASELINE ASSESSMENT
Obtain baseline CBC, BMP, visual acu- uCLASSIFICATION
ity. Obtain negative pregnancy test be- PHARMACOTHERAPEUTIC: Plasma
fore initiating therapy. Question current protein fraction. CLINICAL: Blood
breastfeeding status. Screen for history/ derivative.
co-morbidities, contact lens use. Receive
full medication history, including herbal
products. Assess skin for lesions, ulcers, USES
open wounds. Hypovolemia plasma volume expansion,
maintenance of cardiac output in treat-
INTERVENTION/EVALUATION ment of shock or impending shock.
Monitor renal/hepatic function tests, May be useful in treatment of ovar-
urine output. Encourage PO intake. ian hyperstimulation syndrome, acute/
Assess for hydration status. Offer an- severe nephrosis, cirrhotic ascites, adult
tidiarrheal medication for loose stool. respiratory distress syndrome (ARDS),
Report oliguria, dark or concentrated cardiopulmonary bypass, hemodialysis.
urine. Immediately report skin le- OFF-LABEL: Large-volume paracentesis.
sions, vision changes, dry eye, severe In cirrhotics, with diuretics to help facili-
diarrhea. Obtain chest X-ray if ILD sus- tate diuresis.
pected.
PRECAUTIONS
PATIENT/FAMILY TEACHING
Contraindications: Hypersensitivity to
• Most pts experience diarrhea, and albumin. Pts at risk for volume overload
severe cases may lead to dehydration or (e.g., severe anemia, HF, renal insuffi-
kidney failure; maintain adequate hy- ciency). Dilution with Sterile Water for
dration. • Avoid pregnancy; contra- Injection may cause hemolysis or acute
ception should be used during treat- renal failure. Cautions: Pts for whom
ment and up to 2 wks after sodium restriction is necessary, hepatic/
discontinuation. • Report any yellow- renal failure (added protein load).
ing of skin or eyes, abdominal pain, Avoid 25% concentration in preterm
bruising, black/tarry stools, dark urine, infants (risk of intraventricular hemor-
decreased urine output. • Minimize rhage).
exposure to sunlight. • Immediately
report eye problems (pain, swelling, ACTION
blurred vision, vision changes) or skin Blood volume expander. Therapeutic
blistering/redness. • Do not eat 1 hr Effect: Provides increase in intravascu-
before or 2 hrs after dose. • Do not lar oncotic pressure, mobilizes fluids into
wear contact lenses (may increase risk intravascular space.
of keratitis).

underlined – top prescribed drug


albumin 33
A
PHARMACOKINETICS IV INCOMPATIBILITIES
Route Onset Peak Duration Lipids, micafungin (Mycamine), mid-
IV 15 min (in N/A Dependent on azolam (Versed), vancomycin (Vanco-
well-hy- initial blood cin), verapamil (Isoptin).
drated pt) volume
IV COMPATIBILITIES
Distributed throughout extracellular DiltiaZEM (Cardizem), LORazepam (Ati-
fluid. Half-life: 15–20 days. van).
LIFESPAN CONSIDERATIONS INDICATIONS/ROUTES/DOSAGE
Pregnancy/Lactation: Unknown if b ALERT c 5% should be used in hy-
drug crosses placenta or is distributed in povolemic or intravascularly depleted
breast milk. Children/Elderly: No age- pts. 25% should be used in pts in whom
related precautions noted. fluid and sodium intake must be mini-
mized.
INTERACTIONS
DRUG: None significant. HERBAL: None Usual Dosage
significant. FOOD: None known. LAB IV: ADULTS, ELDERLY: Initially, 25 g; may
VALUES: May increase serum alkaline repeat in 15–30 min if response is inad-
phosphatase. equate.
AVAILABILITY (Rx) Hypovolemia
Injection Solution: (5%): 50 mL, 250 mL, IV: ADULTS, ELDERLY, ADOLESCENTS: 5%
500 mL. (25%): 20 mL, 50 mL, 100 mL. albumin: 12.5–25 g (250–500 mL), re-
peat after 15–30 min, as needed. CHIL-
ADMINISTRATION/HANDLING DREN: 0.5–1 g/kg/dose (10–20 mL/kg/
IV dose of 5% albumin). Repeat in 30-min
intervals as needed.
Reconstitution • A 5% solution may
be made from 25% solution by adding 1 Hemodialysis
volume 25% to 4 volumes 0.9% NaCl IV: ADULTS, ELDERLY:50–100 mL (12.5–
(NaCl preferred). Do not use Sterile Wa- 25 g) of 25% albumin as needed.
ter for Injection (life-threatening hemo-
lysis, acute renal failure can result). Dosage in Renal/Hepatic Impairment
Rate of administration • Give by IV No dose adjustment.
infusion. Rate is variable, depending on
use, blood volume, concentration of solute. SIDE EFFECTS
5%: Do not exceed 2–4 mL/min in pts with Occasional: Hypotension. Rare: High dose
normal plasma volume, 5–10 mL/min in in repeated therapy: altered vital signs,
pts with hypoproteinemia. 25%: Do not chills, fever, increased salivation, nausea,
exceed 1 mL/min in pts with normal vomiting, urticaria, tachycardia.
plasma volume, 2–3 mL/min in pts with
hypoproteinemia. 5% is administered undi- ADVERSE EFFECTS/
luted; 25% may be administered undiluted TOXIC REACTIONS
or diluted in 0.9% NaCl. • May give with- Fluid overload may occur, marked by
out regard to pt blood group or Rh factor. increased B/P, distended neck veins.
Storage • Store at room temperature. Pulmonary edema may occur, evidenced
Appears as clear brownish, odorless, by labored respirations, dyspnea, rales,
moderately viscous fluid. • Do not use wheezing, coughing. Neurologic changes,
if solution has been frozen, appears tur- including headache, weakness, blurred vi-
bid, contains sediment, or if not used sion, behavioral changes, incoordination,
within 4 hrs of opening vial. isolated muscle twitching, may ­occur.
Canadian trade name Non-Crushable Drug High Alert drug
34 albuterol
A
PRECAUTIONS
NURSING CONSIDERATIONS
Contraindications: Hypersensitivity to
BASELINE ASSESSMENT albuterol. Severe hypersensitivity to
Obtain B/P, pulse, respirations imme- milk protein (dry powder inhalation).
diately before administration. Adequate Cautions: Hypertension, cardiovascular
hydration required before albumin is disease, hyperthyroidism, diabetes, HF,
administered. convulsive disorders, glaucoma, hypoka-
lemia, arrhythmias.
INTERVENTION/EVALUATION
Monitor B/P for hypotension/hyperten- ACTION
sion. Assess frequently for evidence of Stimulates beta2-adrenergic receptors
fluid overload, pulmonary edema (see in lungs, resulting in relaxation of bron-
Adverse Effects/Toxic Reactions). chial smooth muscle (little effect on HR).
Check skin for flushing, urticaria. Moni- Therapeutic Effect: Relieves broncho-
tor I&O ratio (watch for decreased out- spasm and reduces airway resistance.
put). Assess for therapeutic response
(increased B/P, decreased edema). PHARMACOKINETICS
Route Onset Peak Duration
PO 15–30 min 2–3 hrs 4–6 hrs
albuterol PO (ex- 30 min 2–4 hrs 12 hrs
tended-
al-bue-ter-ol release)
(Airomir , ProAir HFA, ProAir Inhalation 5–15 min 0.5–2 hrs 2–5 hrs
RespiClick, Proventil HFA, Ventolin Rapidly, well absorbed from GI tract;
HFA, VoSpire ER) rapidly absorbed from bronchi after in-
Do not confuse albuterol with al- halation. Metabolized in liver. Primarily
bumin or atenolol, Proventil with excreted in urine. Half-life: 3.8–6 hrs.
Bentyl, PriLOSEC, or Prinivil, or
Ventolin with Benylin or Vantin. LIFESPAN CONSIDERATIONS
FIXED-COMBINATION(S) Pregnancy/Lactation: Appears to
cross placenta; unknown if distributed
Combivent Respimat: albuterol/ in breast milk. May inhibit uterine con-
ipratropium (a bronchodilator): 100 tractility. Children: Safety and efficacy
mcg/20 mcg per actuation. DuoNeb: not established in pts younger than 2
albuterol/ipratropium 3 mg/0.5 mg. yrs (syrup) or younger than 6 yrs (tab-
uCLASSIFICATION
lets). Elderly: May be more sensitive to
tremor or tachycardia due to age-related
PHARMACOTHERAPEUTIC: Sympa- increased sympathetic sensitivity.
thomimetic (adrenergic beta2-ago-
nist). CLINICAL: Bronchodilator. INTERACTIONS
DRUG: Beta-blockers (e.g., carvedilol,
labetalol, metoprolol) may decrease
USES bronchodilation. MAOIs (e.g., phen-
Treatment or prevention of broncho- elzine, selegiline), linezolid, sym-
spasm due to reversible obstructive pathomimetics (e.g., dopamine,
airway disease, prevention of exercise- norepinephrine) may increase hyper-
induced bronchospasm. OFF-LABEL: tensive effect. HERBAL: None significant.
FOOD: None known. LAB VALUES: May
Treatment of asthma in children under
4 yrs of age. increase blood glucose level. May decrease
serum potassium level.

underlined – top prescribed drug


albuterol 35
A
AVAILABILITY (Rx) YOUNGER: 0.15 mg/kg q20min for 3
Aerosol, Powder Breath Activated Inha- doses (minimum: 2.5 mg), then 0.15–
lation: (ProAir RespiClick): 90 mcg/ 0.3 mg/kg q1–4h as needed. Maxi-
actuation. Aerosol Solution, Inhala- mum: 10 mg q1–4h as needed or 0.5
tion: (ProAir HFA, Proventil HFA, Ven- mg/kg/hr by continuous inhalation.
tolin HFA): 90 mcg/spray. Solution for
Bronchospasm
Nebulization: 0.63 mg/3 mL (0.021%),
PO: ADULTS, CHILDREN OLDER THAN 12
1.25 mg/3 mL (0.042%), 2.5 mg/3 mL
(0.084%), 5 mg/mL (0.5%). Syrup: 2 YRS: 2–4 mg 3–4 times/day. Maxi-
mg/5 mL. Tablets: 2 mg, 4 mg. mum: 8 mg 4 times/day. ELDERLY: 2
mg 3–4 times/day. Maximum: 8 mg 4
Tablets (Extended-Release): 4 mg, times/day. CHILDREN 6–12 YRS: 2 mg 3–4
8 mg. times/day. Maximum: 24 mg/day. CHIL-
ADMINISTRATION/HANDLING DREN 2–5 YRS: 0.1–0.2 mg/kg/dose 3
times/day. Maximum: 4 mg 3 times/day.
PO
PO: (Extended-Release) : ADULTS,
• Do not break, crush, dissolve, or di-
CHILDREN OLDER THAN 12 YRS:4–8 mg
vide extended-release tablets. • Admin-
q12h. Maximum: 32 mg/day. CHILDREN
ister with food.
6–12 YRS: 4 mg q12h. Maximum: 24
Inhalation Aerosol mg/day.
• Shake container well before inhala- Nebulization: ADULTS, ELDERLY, CHIL-
tion. • Prime prior to first use. A spacer DREN 12 YRS AND OLDER: 2.5 mg 3–4
is recommended for use with MDI. times/day as needed. CHILDREN 2–11
• Wait 2 min before inhaling second YRS: (Greater than 15 kg): 0.63–2.5 mg
dose (allows for deeper bronchial pene- 3 to 4 times/day. Maximum: 10 mg/day.
tration). • Rinse mouth with water im- (10–15 kg): 0.63–1.25 mg 3–4 times/
mediately after inhalation (prevents day as needed. Maximum: 10 mg/day.
mouth/throat dryness). Inhalation: ADULTS, ELDERLY, CHILDREN:
2 puffs q4–6h as needed.
Inhalation Powder
• Device is breath activated. • Do not Exercise-Induced Bronchospasm
use with spacer. • Do not wash or put Inhalation: ADULTS, ELDERLY, CHILDREN 5
any part of inhaler to water. YRS AND OLDER: 2 puffs 5 min before ex-
ercise. CHILDREN 4 YRS AND YOUNGER: 1–2
Nebulization puffs 5 min before exercise.
• Administer over 5–15 min.
Dosage in Renal/Hepatic Impairment
INDICATIONS/ROUTES/DOSAGE No dose adjustment.
Acute Bronchospasm, Exacerbation of
Asthma SIDE EFFECTS
Inhalation: ADULTS, ELDERLY, CHILDREN Frequent (27%–4%): Headache, restless-
OLDER THAN 12 YRS: (Acute, Severe):4–8 ness, nervousness, tremors, nausea,
puffs q20min up to 4 hrs, then q1–4h dizziness, throat dryness and irritation,
as needed. CHILDREN 12 YRS AND YOUNGER: pharyngitis, B/P changes including hy-
Acute, Severe: 4–8 puffs q20min for pertension, heartburn, transient wheez-
3 doses, then q1–4h as needed. ing. Occasional (3%–2%): Insomnia,
Nebulization: ADULTS, ELDERLY, CHIL- asthenia, altered taste. Inhalation:
DREN OLDER THAN 12 YRS: Acute, Se- Dry, irritated mouth or throat; cough,
vere: 2.5–5 mg q20min for 3 doses, bronchial irritation. Rare: Drowsiness,
then 2.5–10 mg q1–4h or 10–15 mg/ ­diarrhea, dry mouth, flushing, diaphore-
hr continuously. CHILDREN 12 YRS AND sis, anorexia.

Canadian trade name Non-Crushable Drug High Alert drug


36 alectinib
A
ADVERSE EFFECTS/TOXIC
REACTIONS alectinib
Excessive sympathomimetic stimula-
al-ek-ti-nib
tion may produce palpitations, ectopy,
(Alecensa, Alecensaro )
tachycardia, chest pain, slight increase
Do not confuse alectinib with
in B/P followed by substantial decrease,
afatinib, ibrutinib, imatinib, or
chills, diaphoresis, blanching of skin.
gefitinib.
Too-frequent or excessive use may lead
to decreased bronchodilating effective- uCLASSIFICATION
ness and severe, paradoxical broncho-
PHARMACOTHERAPEUTIC: Tyrosine
constriction.
kinase inhibitor. Anaplastic lymphoma
kinase (ALK) inhibitor. CLINICAL: An-
NURSING CONSIDERATIONS tineoplastic.
BASELINE ASSESSMENT
Assess lung sounds, pulse, B/P, color, USES
characteristics of sputum noted. Of-
Treatment of pts with anaplastic lym-
fer emotional support (high incidence
phoma kinase (ALK)–positive metastatic
of anxiety due to difficulty in breath-
non–small-cell lung cancer (NSCLC).
ing and sympathomimetic response to
drug). PRECAUTIONS
INTERVENTION/EVALUATION Contraindications: Hypersensitivity to
Monitor rate, depth, rhythm, type of alectinib. Cautions: Baseline anemia, leu-
respiration; quality and rate of pulse; kopenia; bradycardia, bradyarrhythmias,
ECG; serum potassium, glucose; ABG chronic edema, diabetes, dehydration,
determinations. Assess lung sounds electrolyte imbalance, hepatic/renal im-
for wheezing (bronchoconstriction), pairment, HF, ocular disease, pulmonary
rales. disease, history of thromboembolism.
PATIENT/FAMILY TEACHING ACTION
• Follow guidelines for proper use of Inhibits ALK. ALK gene abnormalities may
inhaler. • A healthcare provider will result in expression of oncogenic fusion
show you know to properly prepare and proteins, which alter signaling and result in
use your medication. You must demon- increased cellular proliferation/survival in
strate correct preparation and injection tumors. Therapeutic Effect: Inhibition of
techniques before using medica- ALK decreases tumor cell viability.
tion. • Increase fluid intake (decreases
lung secretion viscosity). • Do not take PHARMACOKINETICS
more than 2 inhalations at any one time Metabolized in liver. Protein bind-
(excessive use may produce paradoxical ing: Greater than 99%. Peak plasma
bronchoconstriction or decreased bron- concentration: 4 hrs. Steady state reached
chodilating effect). • Rinsing mouth in 7 days. Excreted in feces (98%), urine
with water immediately after inhalation (less than 0.5%). Half-life: 33 hrs.
may prevent mouth/throat dry-
ness. • Avoid excessive use of caffeine LIFESPAN CONSIDERATIONS
derivatives (chocolate, coffee, tea, cola, Pregnancy/Lactation: Avoid preg-
cocoa). nancy; may cause fetal harm. Females of
reproductive potential should use effective
contraception during treatment and for at
least 1 wk after discontinuation. Unknown

underlined – top prescribed drug


alectinib 37
A
if distributed in breast milk. Breastfeed- bradycardia or to a heart rate of 60 bpm
ing not recommended during treatment or greater, then resume at reduced dose
and for at least 1 wk after discontinuation. level (if pt not taking concomitant medica-
Males with female partners of reproductive tions known to cause bradycardia). Symp-
potential must use barrier methods during tomatic bradycardia in pts taking
treatment and up to 3 mos after discon- concomitant medications known to
tinuation. Children/Elderly: Safety and cause bradycardia: Withhold treatment
efficacy not established. until recovery to asymptomatic bradycar-
dia or heart rate of 60 bpm or greater. If
INTERACTIONS concomitant medication can be adjusted or
DRUG: Beta blockers (e.g., atenolol, discontinued, then resume at same dose. If
carvedilol, metoprolol), calcium concomitant medication cannot be adjusted
channel blockers (e.g., diltiazem, or discontinued, then resume at reduced
verapamil), digoxin may increase dose level. Life-threatening bradycar-
risk of bradycardia. HERBAL: None dia in pts who are not taking concom-
significant. FOOD: High-fat, high- itant medications known to cause
calorie meals increase absorption/ bradycardia: Permanently discontinue.
exposure. LAB VALUES: May increase Life-threatening bradycardia in pts
serum alkaline phosphatase, ALT, AST, who are taking concomitant medi-
bilirubin, CPK, creatinine, glucose. May cations known to cause bradycar-
decrease serum calcium, potassium, dia: Withhold treatment until recovery to
phosphate, sodium; Hgb, Hct, lympho- asymptomatic bradycardia or heart rate of
cytes, RBCs. 60 bpm or greater. If concomitant medica-
tion can be adjusted or discontinued, then
AVAILABILITY (Rx) resume at reduced dose level with frequent
monitoring. Permanently discontinue if bra-
Capsules: 150 mg. dycardia recurs despite dose reduction.
ADMINISTRATION/HANDLING CPK Elevation
PO CPK elevation greater than 5 times
• Give with food. • Administer whole; upper limit of normal (ULN): With-
do not break, crush, cut, or open cap- hold treatment until recovery to baseline
sules. • If a dose is missed or vomiting or less than or equal to 2.5 times ULN,
occurs during administration, give next then resume at same dose. CPK eleva-
dose at regularly scheduled time. tion greater than 10 times ULN or
second occurrence of CPK elevation
INDICATIONS/ROUTES/DOSAGE greater than 5 times ULN: Withhold
Non–Small-Cell Lung Cancer treatment until recovery to baseline or
PO: ADULTS, ELDERLY: 600 mg twice less than or equal to 2.5 times ULN, then
daily until disease progression or unac- resume at reduced dose level.
ceptable toxicity. Hepatotoxicity
Dose Reduction Schedule Serum ALT or AST elevation greater
First dose reduction: 450 mg twice than 5 times ULN with total biliru-
daily. Second dose reduction: 300 mg bin less than or equal to 2 times
twice daily. Permanently discontinue if ULN: Withhold treatment until serum ALT
unable to tolerate 300 mg twice daily. or AST recovers to baseline or less than
or equal to 3 times ULN, then resume at
Dose Modification reduced dose level. Serum ALT or AST
Bradycardia elevation greater than 3 times ULN
Symptomatic bradycardia: Withhold with total serum bilirubin greater
treatment until recovery to asymptomatic than 2 times ULN in the absence of

Canadian trade name Non-Crushable Drug High Alert drug


38 alectinib
A
cholestasis or hemolysis: Perma- s­ erious adverse effects may include endo-
nently discontinue. Total bilirubin eleva- carditis, hemorrhage (unspecified), intes-
tion greater than 3 times ULN: With- tinal perforation, pulmonary embolism.
hold treatment until recovery to baseline
or less than or equal to 1.5 times ULN, then NURSING CONSIDERATIONS
resume at reduced dose level.
BASELINE ASSESSMENT
Pulmonary Obtain baseline CBC, CPK, BMP, LFT; se-
Any grade treatment-related in- rum ionized calcium, phosphate; capil-
terstitial lung disease/pneumoni- lary blood glucose, urine pregnancy, vital
tis: Permanently discontinue. signs. Obtain baseline ECG in pts with
history of arrhythmias, HF, concurrent
Dosage in Renal Impairment
use of medications known to bradycar-
Mild to moderate impairment: No
dia. Question possibility of pregnancy or
dose adjustment. Severe impair-
plans of breastfeeding. Question history
ment: Not specified; use caution.
of hepatic/renal impairment, pulmonary
Dosage in Hepatic Impairment embolism, diabetes, cardiac/pulmonary
Mild impairment: No dose adjustment. disease. Screen for medication known
Moderate to severe impairment: Not to cause bradycardia. Assess visual acu-
specified; use caution. ity. Verify ALK-positive NSCLC test prior to
initiation.
SIDE EFFECTS
INTERVENTION/EVALUATION
Frequent (41%–19%): Fatigue, asthenia,
constipation, edema (peripheral, gen- Monitor CBC routinely; LFTs q2wks dur-
eralized, eyelid, periorbital), myalgia, ing first 2 mos of treatment, then periodi-
musculoskeletal pain, cough, generalized cally thereafter (or more frequently in pts
rash, papular rash, pruritus, macular with hepatic impairment). Obtain BMP,
rash, maculopapular rash, acneiform serum ionized calcium, magnesium if ar-
dermatitis, erythema, nausea. Occa- rhythmia or severe dehydration occurs.
sional (18%–10%): Headache, diarrhea,
Monitor vital signs (esp. heart rate). Ob-
dyspnea, back pain, vomiting, increased tain ECG for bradycardia, chest pain, dys-
weight, blurred vision, vitreous floaters, pnea. Worsening cough, fever, dyspnea
visual impairment, reduced visual acuity, may indicate interstitial lung disease/
asthenopia, diplopia, photosensitivity. pneumonitis. Monitor for hepatotoxicity,
hyperglycemia, vision changes, myalgia,
ADVERSE EFFECTS/TOXIC musculoskeletal pain.
REACTIONS PATIENT/FAMILY TEACHING
Approx. 23% of pts required at least one • Blood levels, ECGs will be monitored
dose reduction. Median time to first dose routinely. • Report history of heart prob-
reduction was 48 days. Decreased Hgb lems including extremity swelling, HF, slow
levels were reported in 56% of pts. Drug- heart rate. Therapy may decrease your
induced hepatotoxicity with elevations of heart rate; report dizziness, chest pain,
serum ALT/AST greater than 5 times ULN palpitations, or fainting. • Worsening
reported in 4%–5% of pts. Most reported cough, fever, or shortness of breath may
cases of hepatotoxicity occurred during indicate severe lung inflammation.
first 2 mos of therapy. Grade 3 interstitial • Avoid pregnancy; contraception recom-
lung disease occurred in less than 1% of mended during treatment and for up to 7
pts. Symptomatic bradycardia reported days after final dose. Do not breastfeed.
in 7.5% of pts. Severe myalgia, musculo- Males with female partners of reproductive
skeletal pain occurred in 29% of pts. CPK potential should use condoms during sex-
elevation occurred in 43% of pts. Other ual activity during treatment and up to
underlined – top prescribed drug
alendronate 39
A
3 mos after final dose. • Blurry vision, PRECAUTIONS
confusion, frequent urination, increased Contraindications: Hypocalcemia, abnor-
thirst, fruity breath may indicate high malities of the esophagus, inability to stand
blood sugar levels. • Report any yellow- or sit upright for at least 30 min, sensitivity
ing of skin or eyes, upper abdominal pain, to alendronate or other bisphosphonates;
bruising, black/tarry stools, dark oral solution or effervescent tablet should
urine. • Do not take newly prescribed not be used in pts at risk for aspiration. Cau-
medication unless approved by doctor tions: Renal impairment, dysphagia, esoph-
who originally started treatment. • Avoid ageal disease, gastritis, ulcers, or duodenitis.
prolonged sun exposure/tanning beds. Use
high SPF sunscreen and lip balm to protect ACTION
against sunburn. • Take with Inhibits bone resorption via actions on os-
food. • Avoid alcohol. teoclasts or osteoclast precursors. Thera-
peutic Effect: Leads to indirect increase
in bone mineral density. Paget’s Disease:
alendronate Inhibits bone resorption, leading to an
indirect decrease in bone formation, but
a-len-dro-nate bone has a more normal architecture.
(Binosto, Fosamax) PHARMACOKINETICS
Do not confuse alendronate
Poorly absorbed after PO administration.
with risedronate, or Fosamax
Protein binding: 78%. After PO admin-
with Flomax.
istration, rapidly taken into bone, with
FIXED-COMBINATION(S) uptake greatest at sites of active bone
turnover. Excreted in urine, feces (as
Fosamax Plus D: alendronate/cho-
unabsorbed drug). Terminal half-life:
lecalciferol (vitamin D analogue):
Greater than 10 yrs (reflects release from
70 mg/2,800 international units, 70
skeleton as bone is resorbed).
mg/5,600 international units.
uCLASSIFICATION
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Possible incom-
PHARMACOTHERAPEUTIC: Bisphos-
plete fetal ossification, decreased maternal
phonate. CLINICAL: Bone resorption
weight gain, delay in delivery. Unknown if
inhibitor, calcium regulator.
distributed in breast milk. Breastfeeding
not recommended. Children: Safety and
USES efficacy not established. Elderly: No age-
related precautions noted.
Fosamax: Treatment of glucocorti-
coid-induced osteoporosis in men and INTERACTIONS
women with low bone mineral density DRUG: Antacids, calcium, iron, magne-
who are receiving at least 7.5 mg pred- sium salts may decrease the concentration/
niSONE (or equivalent). Treatment and effect. Aspirin, NSAIDs (e.g., ibuprofen,
prevention of osteoporosis in males ketorolac, naproxen) may increase ad-
and postmenopausal women. Treat- verse effects (e.g., increased risk of ulcer).
ment of Paget’s disease of the bone in HERBAL: None significant. FOOD: Concur-
pts who are symptomatic, at risk for rent beverages, dietary supplements,
future complications, or with alkaline food may interfere with absorption.
phosphatase equal to or greater than Caffeine may reduce efficacy. LAB VAL-
2 times ULN. Binosto: Treatment of UES: Reduces serum calcium, phosphate.
osteoporosis in males and postmeno- Significant decrease in serum alkaline phos-
pausal women. phatase noted in pts with Paget’s disease.
Canadian trade name Non-Crushable Drug High Alert drug
40 alendronate
A
AVAILABILITY (Rx) 2%): Rash; severe bone, joint, muscle
Solution, Oral: 70 mg/75 mL. Tablets: 5 pain.
mg, 10 mg, 35 mg, 40 mg, 70 mg. Tab-
ADVERSE EFFECTS/TOXIC
lets, Effervescent:(Binosto): 70 mg.
REACTIONS
ADMINISTRATION/HANDLING Overdose produces hypocalcemia, hy-
PO pophosphatemia, significant GI distur-
• Give at least 30 min before first food, bances. Esophageal irritation occurs if
beverage, or medication of the day. Tab- not given with 6–8 oz of plain water or if
lets, effervescent: Dissolve in 4 oz water. pt lies down within 30 min of administra-
Wait at least 5 min after effervescence tion. May increase risk of osteonecrosis
stops. Stir for 10 sec and drink. Oral so- of the jaw.
lution: Follow with at least 2 oz of water.
NURSING CONSIDERATIONS
INDICATIONS/ROUTES/DOSAGE BASELINE ASSESSMENT
Note: Consider discontinuing after 3–5 Obtain baseline serum calcium, phos-
yrs for osteoporosis in pts at low risk for phate, alkaline phosphatase. Hypocal-
fractures. cemia, vitamin D deficiency must be
Osteoporosis (in Men)
corrected before beginning therapy. As-
PO: ADULTS, ELDERLY: 10 mg once daily sess pt’s ability to remain upright for at
in the morning or 70 mg weekly. least 30 minutes.
INTERVENTION/EVALUATION
Glucocorticoid-Induced Osteoporosis
PO: ADULTS, ELDERLY: 5 mg once daily Monitor chemistries (esp. serum cal-
in the morning. POSTMENOPAUSAL cium, phosphorus, alkaline phosphatase
WOMEN NOT RECEIVING ESTROGEN: 10 levels).
mg once daily in the morning. PATIENT/FAMILY TEACHING
Postmenopausal Osteoporosis • Expected benefits occur only when
PO: (Treatment): ADULTS, ELDERLY: 10 medication is taken with full glass (6–8
mg once daily in the morning or 70 oz) of plain water, first thing in the
mg weekly. (Prevention): ADULTS, EL- morning and at least 30 min before first
DERLY: 5 mg once daily in the morning food, beverage, or medication of the day
or 35 mg weekly. is taken. Any other beverage (mineral
water, orange juice, coffee) significantly
Paget’s Disease reduces absorption of medica-
PO: ADULTS, ELDERLY: 40 mg once daily tion. • Do not lie down for at least 30
in the morning for 6 mos. min after taking medication (potentiates
delivery to stomach, reducing risk of
Dosage in Renal Impairment
esophageal irritation). • Report new
Not recommended in pts with creatinine
swallowing difficulties, pain when swal-
clearance less than 35 mL/min.
lowing, chest pain, new/worsening
Dosage in Hepatic Impairment heartburn. • Consider weight-bearing
No dose adjustment. exercises, modify behavioral factors
(e.g., cigarette smoking, alcohol con-
SIDE EFFECTS sumption). • Supplemental calcium
Frequent (8%–7%): Back pain, abdomi- and vitamin D should be taken if dietary
nal pain. Occasional (3%–2%): Nausea, intake inadequate.
abdominal distention, constipation,
diarrhea, flatulence. Rare (less than

underlined – top prescribed drug


alirocumab 41
A
present in breast milk. Children: Safety
alirocumab and efficacy not established. Elderly: No
age-related precautions noted.
al-i-rok-ue-mab
(Praluent) INTERACTIONS
Do not confuse alirocumab with DRUG: May enhance adverse effects/
adalimumab or raxibacumab. toxicity of belimumab. HERBAL: None
significant. FOOD: None known. LAB VAL-
uCLASSIFICATION
UES: Expected to decrease serum LDL-C
PHARMACOTHERAPEUTIC: Propro- levels. May increase serum ALT, AST.
tein convertase subtilisin kexin 9
(PCSK9) inhibitor, monoclonal anti- AVAILABILITY (Rx)
body. CLINICAL: Antihyperlipidemic. Injection Solution: 75 mg/mL, 150 mg/mL
in single-dose, prefilled syringe or pen.
USES ADMINISTRATION/HANDLING
Adjunct to diet, alone or in combination SQ
with other lipid-lowering therapies (e.g., • Visually inspect for particulate matter
statins, ezetimibe) for treatment of primary or discoloration. Solution should ap-
hyperlipidemia (including heterozygous pear clear, colorless to pale yel-
familial hypercholesterolemia [HeFH]) to low. • Allow pen/syringe to warm to
reduce low-density lipoprotein cholesterol room temperature for 30–40 min prior
(LDL-C). To reduce risk of MI, stroke, and to use. • Subcutaneously insert needle
unstable angina requiring hospitalization into abdomen, thigh, or upper arm re-
in adults with established cardiovascular gion and inject solution. It may take up
disease. to 20 sec to fully inject dose. • Do not
inject into areas of active skin disease
PRECAUTIONS
or injury such as sunburns, skin rashes,
Contraindications: Severe hypersensi- inflammation, or skin infections. • Ro-
tivity to alirocumab. Cautions: Hepatic tate injection sites.
impairment. Storage • Refrigerate unused pens/
syringes in outer carton. • Do not
ACTION
freeze. • Discard if pen/syringe has
Prevents binding of PCSK9 to LDL re- been at room temperature more than 24
ceptors on hepatocytes. Increases he- hrs or longer. • Protect from light.
patic uptake of LDL. Therapeutic Ef-
fect: Lowers LDL levels. INDICATIONS/ROUTES/DOSAGE
PHARMACOKINETICS Hyperlipidemia, Secondary Prevention of
Cardiovascular Events
Distributed primarily in circulatory sys-
SQ: ADULTS, ELDERLY: 75 mg once every
tem. Metabolized by protein degrada-
2 wks or 300 mg every 4 wks. May in-
tion into small peptides, amino acids.
crease to maximum dose of 150 mg once
Peak plasma concentration: 3–7 days.
every 2 wks if response inadequate. If a
Steady state reached by 2–3 doses. Half-
dose is missed, administer within 7 days
life: 17–20 days.
of scheduled dose, then resume normal
LIFESPAN CONSIDERATIONS schedule. If missed dose is not within
7 days, wait until next scheduled dose.
Pregnancy/Lactation: May cross pla-
Less frequent dosing: 300 mg q4wks.
cental barrier, esp. during second and
third trimesters. Unknown if distributed in
Dosage in Renal Impairment
breast milk. Human immunoglobulin G is
No dose adjustment.
Canadian trade name Non-Crushable Drug High Alert drug
42 aliskiren
A
Dosage in Hepatic Impairment PATIENT/FAMILY TEACHING
Mild to moderate impairment: No • A healthcare provider will show you
dose adjustment. Severe impairment: how to properly prepare and inject your
Use caution. medication. You must demonstrate cor-
rect preparation and injection techniques
SIDE EFFECTS before using medication. • Treatment
Occasional (11%–7%): Nasopharyngitis, may cause serious allergic reactions such
injection site reactions (e.g., erythema, as itching, hives, rash, or more serious
itching, swelling, pain/tenderness, reactions requiring hospitalization. If al-
bruising/contusion). Rare (5%–2%): Di- lergic reaction occurs, immediately seek
arrhea, bronchitis, myalgia, muscle medical attention. • Do not reuse pre-
spasm, sinusitis, cough, musculoskel- filled pens/syringes.
etal pain.

ADVERSE EFFECTS/TOXIC aliskiren


REACTIONS
Serious hypersensitivity reactions (e.g., a-lis-kye-ren
pruritus, rash, urticaria), including (Rasilez , Tekturna)
some serious events (e.g., hyper- j BLACK BOX ALERT jMay
sensitivity vasculitis, hypersensitivity cause fetal injury, mortality. Dis-
reactions requiring hospitalization), continue as soon as possible once
have been reported. Infections such as pregnancy detected.
UTI (5% of pts) and influenza (6% of Do not confuse Tekturna with
pts) have occurred. Neurologic events Valturna.
such as confusion, memory impair- FIXED-COMBINATION(S)
ment reported in less than 1% of pts.
Immunogenicity (anti-alirocumab Amturnide: aliskiren/amLODIPine
antibodies) reported in 5% of pts. Pts (a calcium channel blocker)/hydro-
who developed neutralizing antibodies CHLOROthiazide (a diuretic): 150
had a higher incidence of injection site mg/5 mg/12.5 mg, 300 mg/5 mg/12.5
reactions. mg, 300 mg/5 mg/25 mg, 300 mg/10
mg/12.5 mg, 300 mg/10 mg/25 mg.
Tekamlo: aliskiren/amLODIPine
NURSING CONSIDERATIONS (a calcium channel blocker): 150
mg/5 mg, 150 mg/10 mg, 300 mg/5
BASELINE ASSESSMENT mg, 300 mg/10 mg. Tekturna HCT:
Obtain baseline LDL-C level, LFT. Ques- aliskiren/hydroCHLOROthiazide (a di-
tion history of hypersensitivity reaction, uretic): 150 mg/12.5 mg, 150 mg/25
hepatic impairment. Assess skin for sun- mg, 300 mg/12.5 mg, 300 mg/25 mg.
burns, skin rashes, inflammation, or skin Valturna: aliskiren/valsartan (an an-
infections. giotensin II receptor antagonist): 150
INTERVENTION/EVALUATION mg/160 mg, 300 mg/320 mg.
Obtain LDL-C level within 4–8 wks after uCLASSIFICATION
treatment initiation or with any dose ti- PHARMACOTHERAPEUTIC: Renin
tration. Monitor for hypersensitivity reac- inhibitor. CLINICAL: Antihypertensive.
tions. If hypersensitivity reaction occurs,
discontinue therapy and treat symptoms
accordingly; monitor until symptoms USES
resolve. Monitor for infections including Treatment of hypertension in adults and
UTI, influenza. children 6 yrs and older (not recom-

underlined – top prescribed drug


aliskiren 43
A
mended as initial treatment). May be products may reduce antihypertensive ef-
used alone or in combination with other fects. Separate by 4 hrs. LAB VALUES: May
antihypertensives. increase serum BUN, creatinine, uric acid,
creatinine kinase, potassium. May decrease
PRECAUTIONS Hgb, Hct.
Contraindications: Hypersensitivity to
aliskiren. Concurrent use with ACE inhibi- AVAILABILITY (Rx)
tor or Angiotensin II Receptor Blockers in Tablets, Film-Coated: 150 mg, 300 mg.
pts with diabetes. Children younger than
2 yrs. Cautions: Severe renal impairment. ADMINISTRATION/HANDLING
History of angioedema, dialysis, nephrotic PO
syndrome, renovascular hypertension. • High-fat meals substantially decrease
Concurrent use with P-glycoprotein in- absorption. • Consistent administra-
hibitors (e.g., cycloSPORINE). tion with regard to meals is recommen­
ded. • Do not break, crush, dissolve,
ACTION or divide film-coated tablets.
Direct renin inhibitor. Decreases plasma
renin activity (PRA), inhibiting the con- INDICATIONS/ROUTES/DOSAGE
version of angiotensinogen to angiotensin Hypertension
I, decreasing the formation of angiotensin PO: ADULTS, ELDERLY: Initially, 150 mg/
II. Therapeutic Effect: Reduces B/P. day. May increase to 300 mg/day. CHIL-
DREN WEIGHING 20–50 KG: 75 mg once
PHARMACOKINETICS daily. Maximum: 150 mg/day.
Peak plasma concentration reached Dosage in Renal Impairment
within 1–3 hrs. Protein binding: 49%. Mild to moderate impairment: No
Metabolized in liver. Minimally excreted dose adjustment. Severe impairment:
in urine. Peak plasma steady-state levels Use caution.
reached in 7–8 days. Half-life: 24 hrs.
Dosage in Hepatic Impairment
LIFESPAN CONSIDERATIONS No dose adjustment.
Pregnancy/Lactation: Carcinogenic SIDE EFFECTS
potential to fetus. May cause fetal/neona-
tal morbidity, mortality. Unknown if dis- Rare (2%–1%): Diarrhea, particularly in
tributed in breast milk. Children: Safety women, elderly (older than 65 yrs), gas-
and efficacy not established. Elderly: No troesophageal reflux, cough, rash.
age-related precautions noted. ADVERSE EFFECTS/TOXIC
INTERACTIONS REACTIONS
DRUG: CycloSPORINE, itraconazole Angioedema, periorbital edema, edema
may increase concentration/effect. Angio- of hands, generalized edema have been
tensin-converting enzymes (ACE) in- reported.
hibitors (e.g., enalapril, lisinopril), an- NURSING CONSIDERATIONS
giotensin II receptor blockers (ARBs)
(e.g., losartan, valsartan) may increase BASELINE ASSESSMENT
risk of hyperkalemia. HERBAL: Herb- Correct hypovolemia in pts on concur-
als with hypotensive properties (e.g., rent diuretic therapy. Obtain B/P and
black cohosh, garlic) may increase ef- apical pulse immediately before each
fect. Herbals with hypertensive prop- dose, in addition to regular monitoring
erties (e.g., ephedra, yohimbe) may (be alert to fluctuations). If excessive re-
decrease effect. FOOD: High-fat meals sub- duction in B/P occurs, place pt in supine
stantially decrease absorption. Grapefruit position, feet slightly elevated.

Canadian trade name Non-Crushable Drug High Alert drug


44 allopurinol
A
INTERVENTION/EVALUATION ACTION
Assess for edema. Monitor I&O; weigh Decreases uric acid production by in-
daily. Monitor B/P, renal function tests, hibiting xanthine oxidase, an enzyme re-
potassium, Hgb, Hct. sponsible for converting xanthine to uric
PATIENT/FAMILY TEACHING acid. Therapeutic Effect: Reduces uric
acid concentrations in serum and urine.
• Pregnant pts should avoid second- and
third-trimester exposure to aliskiren. • Re- PHARMACOKINETICS
port swelling of face/lips/tongue, difficulty
breathing. • Avoid stren­uous exercise dur- Route Onset Peak Duration
ing hot weather (risk of dehydration, hypo- PO, IV 2–3 days 1–3 wks 1–2 wks
tension). • Do not chew, crush, dissolve,
Well absorbed from GI tract. Widely dis-
or divide film-coated tablets.
tributed. Protein binding: less than 1%.
Metabolized in liver. Excreted primarily
in urine. Removed by hemodialysis. Half-
allopurinol life: 1–3 hrs; metabolite, 12–30 hrs.
al-oh-pure-i-nol LIFESPAN CONSIDERATIONS
(Aloprim, Zyloprim) Pregnancy/Lactation: Unknown if
Do not confuse allopurinol with drug crosses placenta or is distributed in
Apresoline or haloperidol, or Zy- breast milk. Children/Elderly: No age-
loprim with Zorprin or Zovirax. related precautions noted.
FIXED-COMBINATION(S) INTERACTIONS
Duzallo: allopurinol/lesinurad (uric DRUG: Angiotensin-converting en-
acid transporter-1 inhibitor): 200 zyme (ACE) inhibitors (e.g., enala-
mg/200 mg, 300 mg/200 mg. pril, lisinopril) may increase potential
uCLASSIFICATION for allergic or hypersensitivity reactions.
Antacids may decrease absorption. May
PHARMACOTHERAPEUTIC: Xanthine increase concentration/effects of azaTHI-
oxidase inhibitor. CLINICAL: anti-gout Oprine, didanosine, mercaptopurine.
May increase adverse effects of pegloti-
USES case. May increase anticoagulant effect
of vitamin K antagonists (e.g., warfa-
PO: Management of primary or second- rin). May decrease concentration/effect of
ary gout (e.g., acute attack, nephropathy). capecitabine. HERBAL: None significant.
Treatment of secondary hyperuricemia that FOOD: None known. LAB VALUES: May
may occur during cancer treatment. Man- increase serum BUN, alkaline phosphatase,
agement of recurrent uric acid and calcium ALT, AST, creatinine.
oxalate calculi. Injection: Management
of elevated uric acid in cancer treatment AVAILABILITY (Rx)
for leukemia, lymphoma, or solid tumor Injection, Powder for Reconstitution:
malignancies. (Aloprim): 500 mg. Tablets: (Zy-
PRECAUTIONS loprim): 100 mg, 300 mg.

Contraindications: Severe hypersensi- ADMINISTRATION/HANDLING


tivity to allopurinol. Cautions: Renal/
hepatic impairment; pts taking diuretics, IV
mercaptopurine or azaTHIOprine, other Reconstitution • Reconstitute 500-mg
drugs causing myelosuppression. Do not vial with 25 mL Sterile Water for Injection
use in asymptomatic hyperuricemia. (concentration of 20 mg/mL). • Further
underlined – top prescribed drug
allopurinol 45
A
dilute with 0.9% NaCl or D5W (50–100 severe: 400–600 mg/day in 2–3 di-
mL) to a concentration of 6 mg/mL or less. vided doses. Maximum: 800 mg/day.
Rate of administration • Infuse over
15–60 min. Daily doses can be given as a Secondary Hyperuricemia Associated
single infusion or in equally divided with Chemotherapy
doses at 6-, 8-, or 12-hr intervals. PO: ADULTS, CHILDREN OLDER THAN 10
Storage • Solution should appear YRS: 600–800 mg/day in 2–3 divided
clear and colorless. • Store unreconsti- doses for 2–3 days starting 1–2 days
tuted vials at room temperature. • Do before chemotherapy. CHILDREN 6–10
not refrigerate reconstituted and/or di- YRS: 300 mg/day in 2–3 divided doses.
luted solution. Must administer within 10 CHILDREN YOUNGER THAN 6 YRS: 150 mg/
hrs of preparation. • Do not use if pre- day in 3 divided doses.
cipitate forms or solution is discolored. b ALERT c IV: Daily dose can be given
as single infusion or at 6-, 8-, or 12-hr
PO intervals.
• Give after meals with plenty of fluid. IV: ADULTS, ELDERLY, CHILDREN 10 YRS
• Fluid intake should yield slightly alka- OR OLDER: 200–400 mg/m2/day begin-
line urine and output of approximately ning 24–48 hrs before initiation of che-
2 L in adults. • Dosages greater than motherapy. CHILDREN YOUNGER THAN 10
300 mg/day to be administered in ­divided YRS: 200 mg/m2/day beginning 24–48
doses. hrs before initiation of chemotherapy.
Maximum: 600 mg/day.
IV INCOMPATIBILITIES
Amikacin (Amikin), carmustine (BiCNU), Recurrent Uric Acid Calcium Oxalate
cefotaxime (Claforan), clindamycin (Cleo- Calculi
cin), cytarabine (Ara-C), dacarbazine PO: ADULTS: 200–300 mg/day in single
(DTIC), diphenhydrAMINE (Benadryl), or divided doses.
DOXOrubicin (Adriamycin), doxycycline
(Vibramycin), gentamicin, haloperidol Dosage in Renal Impairment
(Haldol), hydrOXYzine (Vistaril), IDA- Dosage is modified based on creatinine
rubicin (Idamycin), imipenem-cilastatin clearance. PO: Removed by hemodialy-
(Primaxin), methylPREDNISolone (SOLU- sis. Administer dose following hemodialy-
Medrol), metoclopramide (Reglan), on- sis or administer 50% supplemental dose.
dansetron (Zofran), streptozocin (Zano-
sar), tobramycin, vinorelbine (Navelbine). IV/PO
Creatinine
IV COMPATIBILITIES
Clearance Dosage
Bumetanide (Bumex), calcium gluco- 10–20 mL/min 200 mg/day
nate, furosemide (Lasix), heparin, HY- 3–9 mL/min 100 mg/day
DROmorphone (Dilaudid), LORazepam Less than 100 mg at extended inter-
(Ativan), morphine, potassium chloride. 3 mL/min vals
HD 100 mg q48h (increase
INDICATIONS/ROUTES/DOSAGE cautiously to 300 mg)
b ALERT c Doses greater than 300 mg
should be given in divided doses. Dosage in Hepatic Impairment
No dose adjustment.
Gout
PO: ADULTS, ELDERLY: Initially, 100 mg/ SIDE EFFECTS
day. Increase at weekly intervals needed Occasional: PO: Drowsiness, unusual
to achieve desired serum uric acid level. hair loss. IV: Rash, nausea, vomiting.
Mild: 200–300 mg/day. Moderate to Rare: Diarrhea, headache.

Canadian trade name Non-Crushable Drug High Alert drug


46 almotriptan
A
ADVERSE EFFECTS/ USES
TOXIC REACTIONS Acute treatment of migraine headache
Pruritic maculopapular rash, possibly ac- with or without aura in adults. Acute
companied by malaise, fever, chills, joint treatment of migraine headache in ado-
pain, nausea, vomiting should be consid- lescents 12–17 yrs with history of mi-
ered a toxic reaction. Severe hypersensi- graine with or without aura and having
tivity reaction may follow appearance of attacks usually lasting 4 or more hrs
rash. Bone marrow depression, hepato- when left untreated.
toxicity, peripheral neuritis, acute renal
failure occur rarely. PRECAUTIONS
Contraindications: Hypersensitivity to almo-
NURSING CONSIDERATIONS triptan. Cerebrovascular disease (e.g., recent
BASELINE ASSESSMENT stroke, transient ischemic attacks), periph-
eral vascular disease (e.g., ischemic bowel
Obtain baseline BMP, LFT. Instruct pt to disease), hemiplegic or basilar migraine,
drink minimum of 2,500–3,000 mL of ischemic heart disease (including angina
fluid daily while taking medication. pectoris, history of MI, silent ischemia, and
INTERVENTION/EVALUATION Prinzmetal’s angina), uncontrolled hyper-
Discontinue medication immediately if tension, use within 24 hrs of ergotamine-
rash or other evidence of allergic reaction containing preparations or another 5-HT1B
occurs. Monitor I&O (output should be at agonist. Cautions: Mild to moderate renal
least 2,000 mL/day). Assess serum chem- or hepatic impairment, pt profile suggesting
istries, uric acid, hepatic function. Assess cardiovascular risks, controlled hyperten-
urine for cloudiness, unusual color, odor. sion; history of CVA, sulfonamide allergy.
Gout: Assess for therapeutic response: ACTION
relief of pain, stiffness, swelling; increased
joint mobility; reduced joint tenderness; Binds selectively to serotonin recep-
improved grip strength. tors in cranial arteries producing a
vasoconstrictive effect. Decreases in-
PATIENT/FAMILY TEACHING flammation associated with relief of
• May take 1 wk or longer for full migraine. Therapeutic Effect: Pro-
­ther­apeutic effect. • Maintain adequate duces relief of migraine headache.
­hydration; drink 2,500–3,000 mL of fluid
daily while taking medication. • Avoid PHARMACOKINETICS
tasks that require alertness, motor skills Well absorbed after PO administration.
until response to drug is established. • Protein binding: 35%. Metabolized by
Avoid alcohol (may increase uric acid). liver. Primarily excreted in urine. Half-
life: 3–4 hrs.

almotriptan LIFESPAN CONSIDERATIONS


Pregnancy/Lactation: Unknown
al-moe-trip-tan if distributed in breast milk. Chil-
(Axert) dren: Safety and efficacy not established
Do not confuse almotriptan with in pts younger than 12 yrs. Elderly: No
alvimopan, or Axert with Antivert. age-related precautions noted.
uCLASSIFICATION
INTERACTIONS
PHARMACOTHERAPEUTIC: Seroto- DRUG: Ergot derivatives (e.g., di-
nin receptor agonist (5-HT1B). CLINI- hydroergotamine, ergotamine) may
CAL: Antimigraine.
increase vasoconstrictive effect. Strong
underlined – top prescribed drug
ALPRAZolam 47
A
CYP3A4 inhibitors (e.g., clarithromy- arrhythmias occur rarely but particularly
cin, ketoconazole, ritonavir) may in- in pts with hypertension, diabetes, obesity,
crease concentration/effect. MAOIs (e.g., smokers, and those with strong family his-
phenelzine, selegiline) may increase tory of coronary artery disease.
concentration/effect. HERBAL: None sig-
nificant. FOOD: None known. LAB VAL- NURSING CONSIDERATIONS
UES: None significant. BASELINE ASSESSMENT
AVAILABILITY (Rx) Question for history of peripheral vas-
Tablets: 6.5 mg, 12.5 mg. cular disease, cardiac conduction disor-
ders, CVA. Question pt regarding onset,
ADMINISTRATION/HANDLING location, duration of migraine, and pos-
PO
sible precipitating factors.
• Swallow whole; do not break, crush, INTERVENTION/EVALUATION
dissolve, or divide tablets. • Take with Evaluate for relief of migraine headache
full glass of water. • May give without and associated photophobia, phonopho-
regard to food. bia (sound sensitivity), nausea, vomiting.
INDICATIONS/ROUTES/DOSAGE PATIENT/FAMILY TEACHING
Migraine Headache • Take a single dose as soon as symptoms
PO: ADULTS, ELDERLY, ADOLESCENTS 12– of an actual migraine attack ap-
17 YRS: Initially, 6.25–12.5 mg as a sin- pear. • Medication is intended to relieve
gle dose. If headache returns, dose may migraine, not to prevent or reduce num-
be repeated after 2 hrs. Maximum: 2 ber of attacks. • Lie down in quiet, dark
doses/24 hrs (25 mg). room for additional benefit after taking
medication. • Avoid tasks that require
Concurrent Use of CYP3A4 Inhibitors
alertness, motor skills until response to
ADULTS, ELDERLY: Recommended initial drug is established. • Report immedi-
dose is 6.25 mg, maximum daily dose is ately if palpitations, pain or tightness in
12.5 mg. Avoid use in pts with renal or chest or throat, or pain or weakness of
hepatic impairment AND use of CYP3A4 extremities occurs. • Swallow whole; do
inhibitors. not chew, crush, dissolve, or divide tablets.
Dosage in Renal Impairment
Creatinine clearance 30 mL/min or
less: Initially, 6.25 mg in a single dose.
Maximum: 12.5 mg/day. ALPRAZolam
Dosage in Hepatic Impairment
Initially, 6.25 mg in a single dose. Maxi- al-praz-oh-lam
mum: 12.5 mg/day. (ALPRAZolam Intensol, ALPRAZolam
XR, Apo-Alpraz , Xanax, Xanax
SIDE EFFECTS XR)
Rare (2%–1%): Nausea, dry mouth, head- Do not confuse ALPRAZolam
ache, dizziness, somnolence, paresthe- with LORazepam, or Xanax with
sia, flushing. Tenex, Tylox, Xopenex, Zantac,
or ZyrTEC.
ADVERSE EFFECTS/
uCLASSIFICATION
TOXIC REACTIONS
Excessive dosage may produce tremor, red- PHARMACOTHERAPEUTIC: Ben-
ness of extremities, decreased ­respirations, zodiazepine (Schedule IV). CLINI-
cyanosis, seizures, chest pain. Serious CAL: Antianxiety.

Canadian trade name Non-Crushable Drug High Alert drug


48 ALPRAZolam
A
USES inhibitors (e.g., clarithromycin, ke-
Management of generalized anxiety dis- toconazole, ritonavir) may increase
orders (GAD). Short-term relief of symp- concentration/effect. Strong CYP3A4
toms of anxiety, panic disorder, with or inducers (e.g., carbamazepine, phe-
without agoraphobia. Anxiety associated nytoin, rifampin) may decrease con-
with depression. OFF-LABEL: Anxiety in centration/effect. HERBAL: Herbals with
children. Preoperative anxiety. sedative properties (e.g., chamo-
mile, kava kava, valerian) may in-
PRECAUTIONS crease CNS depression. St. John’s wort
Contraindications: Hypersensitivity to AL- may decrease effects. FOOD: Grapefruit
PRAZolam. Acute narrow angle-closure products may increase level, effects.
glaucoma, concurrent use with keto- LAB VALUES: None significant.
conazole or itraconazole or other potent
AVAILABILITY (Rx)
CYP3A4 inhibitors. Cautions: Renal/he-
patic impairment, predisposition to urate Solution, Oral: (Alprazolam Intensol): 1
nephropathy, obese pts. Concurrent use mg/mL. Tablets (Orally Disintegrating):
of CYP3A4 inhibitors/inducers and major 0.25 mg, 0.5 mg, 1 mg, 2 mg. Tablets
CYP3A4 substrates; debilitated pts, respi- (Immediate-Release): (Xanax): 0.25 mg,
ratory disease, depression (esp. suicidal 0.5 mg, 1 mg, 2 mg.
risk), elderly (increased risk of severe Tablets (Extended-Release): (Xanax
toxicity). History of substance abuse. XR): 0.5 mg, 1 mg, 2 mg, 3 mg.

ACTION ADMINISTRATION/HANDLING
Enhances the inhibitory effects of the PO, Immediate-Release
neurotransmitter gamma-aminobutyric • May give without regard to
acid in the brain. Therapeutic Ef- food. • Tablets may be crushed. • If
fect: Produces anxiolytic effect due to oral intake is not possible, may be given
CNS depressant action. sublingually.
PHARMACOKINETICS PO, Extended-Release
• Administer once daily. • Do not
Well absorbed from GI tract. Protein bind-
break, crush, dissolve, or divide extended-
ing: 80%. Metabolized in liver. Primarily
release tablets. Swallow whole.
excreted in urine. Minimal removal by
hemodialysis. Half-life: 6–27 hrs. PO, Orally Disintegrating
• Place tablet on tongue, allow to dis-
LIFESPAN CONSIDERATIONS solve. • Swallow with saliva. • Admin-
Pregnancy/Lactation: Crosses pla- istration with water not necessary. • If
centa; distributed in breast milk. Chronic using ½ tab, discard remaining ½ tab.
ingestion during pregnancy may produce
withdrawal symptoms, CNS depression in INDICATIONS/ROUTES/DOSAGE
neonates. Children: Safety and efficacy Anxiety Disorders
not established. Elderly: Use small ini- PO: (Immediate-Release, Oral Con-
tial doses with gradual increase to avoid centrate, ODT): ADULTS: Initially, 0.25–
ataxia (muscular incoordination) or ex- 0.5 mg 3 times/day. May titrate q3–4days.
cessive sedation. May have increased risk Maximum: 4 mg/day in divided doses.
of falls, delirium. CHILDREN, YOUNGER THAN 18 YRS: 0.125
mg 3 times/day. May increase by 0.125–
INTERACTIONS 0.25 mg/dose. Maximum: 0.06 mg/kg/
DRUG: CNS depressants (e.g., alco- day or 0.02 mg/kg/dose. Range: 0.375–3
hol, morphine, zolpidem) may in- mg/day. ELDERLY, DEBILITATED PTS, PTS
crease CNS depression. Strong CYP3A4 WITH HEPATIC DISEASE OR LOW SERUM

underlined – top prescribed drug


alteplase 49
A
ALBUMIN: Initially, 0.25 mg 2–3 times/ d­ iminished reflexes, coma. Blood dyscra-
day. Gradually increase to optimum ther- sias noted rarely. Antidote: Flumazenil
apeutic response. (see Appendix J for dosage).
Anxiety with Depression
NURSING CONSIDERATIONS
PO: ADULTS: (average dose required)
2.5–3 mg/day in divided doses. BASELINE ASSESSMENT

Panic Disorder Assess degree of anxiety; assess for


PO: (Immediate-Release, Oral Con- drowsiness, dizziness, light-headedness.
centrate, ODT): ADULTS: Initially, 0.5 Assess motor responses (agitation, trem-
mg 3 times/day. May increase at 3- to 4-day bling, tension), autonomic responses
intervals in increments of 1 mg or less a (cold/clammy hands, diaphoresis). Initi-
day. Range: 5–6 mg/day. Maximum: 10 ate fall precautions.
mg/day. ELDERLY: Initially, 0.125–0.25 mg INTERVENTION/EVALUATION
twice daily. May increase in 0.125-mg in- For pts on long-term therapy, perform he-
crements until desired ­effect attained. patic/renal function tests, CBC periodically.
PO: (Extended-Release):
Assess for paradoxical reaction, particu-
b ALERT c To switch from immediate-­
larly during early therapy. Evaluate for ther-
release to extended-release form, give total apeutic response: calm facial expression,
daily dose (immediate-release) as a single decreased restlessness, insomnia. Monitor
daily dose of extended-release form. respiratory and cardiovascular status.
ADULTS: Initially, 0.5–1 mg once daily.
May titrate at 3- to 4-day intervals. Range: PATIENT/FAMILY TEACHING
3–6 mg/day. ELDERLY: Initially, 0.5 mg • Drowsiness usually disappears during
once daily. continued therapy. • If dizziness occurs,
Dosage in Renal Impairment change positions slowly from recumbent
No dose adjustment. to sitting position before stand-
ing. • Avoid tasks that require alertness,
Dosage in Hepatic Impairment motor skills until response to drug is es-
Severe disease: (Immediate-Release): tablished. • Smoking reduces drug ef-
0.25 mg 2–3 mg times/day. (Extended- fectiveness. • Sour hard candy, gum,
Release): 0.5 mg once daily. sips of water may relieve dry mouth. • Do
not abruptly withdraw medication after
SIDE EFFECTS long-term therapy. • Avoid alcohol.
Frequent (41%–20%): Ataxia, light-head- • Do not take other medications without
edness, drowsiness, slurred speech (par- consulting physician.
ticularly in elderly or debilitated pts).
Occasional (15%–5%): Confusion, depres-
sion, blurred vision, constipation, diarrhea,
dry mouth, headache, nausea. Rare (4% or
alteplase
less): Behavioral problems such as anger, al-te-plase
impaired memory; paradoxical reactions (Activase, Cathflo Activase)
(insomnia, nervousness, irritability). Do not confuse alteplase or
ADVERSE EFFECTS/ Activase with Altace, or Activase
TOXIC REACTIONS with Cathflo Activase.
Abrupt or too-rapid withdrawal may result uCLASSIFICATION
in restlessness, irritability, insomnia, hand PHARMACOTHERAPEUTIC: Tissue
tremors, abdominal/muscle cramps, plasminogen activator (tPA). CLINI-
diaphoresis, vomiting, seizures. Over- CAL: Thrombolytic.
dose results in drowsiness, ­confusion,
Canadian trade name Non-Crushable Drug High Alert drug
50 alteplase
A
USES INTERACTIONS
Treatment of ST-elevation MI (STEMI) DRUG: Heparin, low molecular
for lysis of thrombi in coronary arter- weight heparins, medications alter-
ies, acute ischemic stroke (AIS), acute ing platelet function (e.g., clopi-
massive pulmonary embolism (PE). dogrel, NSAIDs, thrombolytics),
Treatment of occluded central venous oral anticoagulants (e.g., warfarin)
catheters. OFF-LABEL: Acute periph- increase risk of bleeding. May increase
eral occlusive disease, prosthetic valve anticoagulant effect of desirudin.
thrombosis. Acute ischemic stroke HERBAL: Herbals with anticoagulant/
presenting 3–4½ hrs after onset of antiplatelet properties (e.g., garlic,
symptoms. ginger, ginkgo biloba) may increase
adverse effects. FOOD: None known. LAB
PRECAUTIONS VALUES: Decreases plasminogen, fibrin-
Contraindications: Hypersensitivity to ogen levels during infusion, decreases
alteplase. Active internal bleeding, AV clotting time (confirms the presence of
malformation or aneurysm, bleeding lysis). May decrease Hgb, Hct.
diathesis CVA, intracranial neoplasm,
intracranial or intraspinal surgery or AVAILABILITY (Rx)
trauma, recent (within past 2 mos), Injection, Powder for Reconstitution:
severe uncontrolled hypertension, sus- (Cathflo Activase): 2 mg, (Activase):
pected aortic dissection. Cautions: Re- 50 mg, 100 mg.
cent (within 10 days) major surgery
or GI bleeding, OB delivery, organ bi- ADMINISTRATION/HANDLING
opsy, recent trauma or CPR, left heart IV
thrombus, endocarditis, severe hepatic
disease, pregnancy, elderly, cerebro- Reconstitution • Activase: Reconsti-
vascular disease, diabetic retinopathy, tute immediately before use with Sterile
thrombophlebitis, occluded AV cannula Water for Injection. • Reconstitute
at infected site. 100-mg vial with 100 mL Sterile Water
for Injection (50-mg vial with 50 mL
ACTION sterile water) without preservative to
Binds to fibrin in a thrombus and con- provide a concentration of 1 mg/
verts entrapped plasminogen to plasmin, mL. • Activase Cathflo: Add 2.2 mL
initiating local fibrinolysis. Therapeutic Sterile Water for Injection to provide
Effect: Degrades fibrin clots, fibrino- concentration of 1 mg/mL. • Avoid ex-
gen, other plasma proteins. cessive agitation; gently swirl or slowly
invert vial to reconstitute.
Rate of administration • Activase:
PHARMACOKINETICS
Give by IV infusion via infusion pump
Rapidly metabolized in liver. Primarily (see Indications/Routes/Dosage). • If
excreted in urine. Half-life: 35 min. minor bleeding occurs at puncture sites,
apply pressure for 30 sec; if unrelieved,
LIFESPAN CONSIDERATIONS apply pressure dressing. • If uncon-
Pregnancy/Lactation: Use only when trolled hemorrhage occurs, discontinue
benefit outweighs potential risk to fe- infusion immediately (slowing rate of
tus. Unknown if drug crosses placenta infusion may produce worsening
or is distributed in breast milk. Chil- ­hemorrhage). • Avoid undue pressure
dren: Safety and efficacy not estab- when drug is injected into catheter
lished. Elderly: May have increased risk (can rupture catheter or expel clot
of bleeding; monitor closely. into circulation). • Instill dose into

underlined – top prescribed drug


alteplase 51
A
­occluded catheter. • After 30 min, as- IV infusion: ADULTS WEIGHING 100 KG
sess catheter function by attempting to OR LESS: 0.09 mg/kg as IV bolus over
aspirate blood. • If still occluded, let 1 min, then 0.81 mg/kg as continuous
dose dwell an additional 90 min. • If infusion over 60 min. WEIGHING MORE
function not restored, a second dose may THAN 100 KG: 9 mg bolus over 1 min,
be instilled. then 81 mg as continuous infusion over
Storage • Activase: Store vials at 60 min.
room temperature. • After reconstitu-
Central Venous Catheter Clearance
tion, solution appears colorless to pale
IV: ADULTS, ELDERLY: Up to 2 mg; may
yellow. • Solution is stable for 8 hrs after
reconstitution. Discard unused portions. repeat after 2 hrs. If catheter functional,
withdraw 4–5 mL blood to remove drug
IV INCOMPATIBILITIES and residual clot.
DOBUTamine (Dobutrex), DOPamine Usual Neonatal Dosage
(Intropin), heparin. Occluded IV catheter: Use 1 mg/mL
conc (maximum: 2 mg/2 mL) leave in
IV COMPATIBILITIES lumen up to 2 hrs, then aspirate.
Lidocaine, metoprolol (Lopressor), Systemic thrombosis: 0.1–0.6 mg/kg/
morphine, nitroglycerin, propranolol hr for 6 hrs. Usual dose: 0.5 mg/kg/hr.
(Inderal).
Dosage in Renal/Hepatic Impairment
INDICATIONS/ROUTES/DOSAGE No dose adjustment.
Acute MI
IV infusion: ADULTS WEIGHING MORE SIDE EFFECTS
THAN 67 KG: Total dose: 100 mg over Frequent: Superficial bleeding at puncture
90 min, starting with 15-mg bolus over sites, decreased B/P. Occasional: Allergic
1–2 min, then 50 mg over 30 min, then reaction (rash, wheezing, bruising).
35 mg over 60 min. ADULTS WEIGHING
67 KG OR LESS: Total dose: Start with ADVERSE EFFECTS/TOXIC
15-mg bolus over 1–2 min, then 0.75 REACTIONS
mg/kg over 30 min (maximum: 50 Severe internal hemorrhage, intracranial
mg), then 0.5 mg/kg over 60 min hemorrhage may occur. Lysis of coronary
(maximum: 35 mg). Maximum to- thrombi may produce atrial or ventricu-
tal dose: 100 mg. lar arrhythmias or stroke.
Acute Pulmonary Emboli NURSING CONSIDERATIONS
IV infusion: ADULTS: 100 mg over 2
hrs. May give as a 10-mg bolus followed BASELINE ASSESSMENT
by 90 mg over 2 hrs. Institute or rein- Assess for contraindications to therapy.
stitute heparin near end or immediately Obtain baseline B/P, apical pulse. Record
after infusion when activated partial weight. Evaluate 12-lead ECG, cardiac
thromboplastin time (aPTT) or throm- enzymes, electrolytes. Assess Hct, platelet
bin time (TT) returns to twice normal count, thrombin time (TT), prothrombin
or less. time (PT), activated partial thromboplastin
time (aPTT), fibrinogen level before ther-
Acute Ischemic Stroke
apy is instituted. Type and screen blood.
b ALERT c Dose should be given within
the first 3 hrs of the onset of symptoms. INTERVENTION/EVALUATION
Recommended total dose: 0.9 mg/kg. Perform continuous cardiac monitor-
Maximum: 90 mg. ing for arrhythmias. Check B/P, pulse,

Canadian trade name Non-Crushable Drug High Alert drug


52 amikacin
A
respirations q15min until stable, then tant use of neurotoxic or nephrotoxic
hourly. Check peripheral pulses, heart medications.
and lung sounds. Monitor for chest
pain relief and notify physician of con- ACTION
tinuation or recurrence (note location, Inhibits protein synthesis in susceptible
type, intensity). Assess for bleeding: bacteria by binding to 30S ribosomal
overt blood, occult blood in any body unit. Therapeutic Effect: Interferes
substance. Monitor aPTT per protocol. with protein synthesis of susceptible mi-
Maintain B/P; avoid any trauma that croorganisms.
might increase risk of bleeding (e.g.,
injections, shaving). Assess neurologic PHARMACOKINETICS
status frequently. Rapid, complete absorption after IM
administration. Protein binding: 0%–
10%. Widely distributed (penetrates
blood-brain barrier when meninges
amikacin are inflamed). Excreted unchanged in
urine. Removed by hemodialysis. Half-
am-i-kay-sin life: 2–4 hrs (increased in renal im-
(Amikin ) pairment, neonates; decreased in cystic
j BLACK BOX ALERT jMay fibrosis, burn pts, febrile pts).
cause neurotoxicity, nephrotoxicity,
and/or neuromuscular blockade LIFESPAN CONSIDERATIONS
and respiratory paralysis. Ototoxic- Pregnancy/Lactation: Readily crosses
ity usually is irreversible; nephro-
toxicity usually is reversible. placenta; small amounts distributed in
Do not confuse amikacin or breast milk. May produce fetal nephro-
Amikin with Amicar, or amika- toxicity. Children: Neonates, prema-
cin with anakinra. ture infants may be more susceptible to
toxicity due to immature renal function.
uCLASSIFICATION Elderly: Higher risk of toxicity due to
PHARMACOTHERAPEUTIC: Amino- age-related renal impairment, increased
glycoside. CLINICAL: Antibiotic. risk of hearing loss.
INTERACTIONS
USES DRUG: Foscarnet, mannitol may in-
crease nephrotoxic effect. Penicillin may
Treatment of serious infections (e.g., bone decrease concentration/effect. HERBAL:
infections, respiratory tract infections, None significant. FOOD: None known.
septicemia) due to Pseudomonas, other LAB VALUES: May increase serum creati-
gram-negative organisms (Proteus, Ser­ nine, BUN, ALT, AST, bilirubin, LDH. May
ratia, E. coli, Enterobacter, Klebsiella). decrease serum calcium, magnesium,
OFF-LABEL: Mycobacterium avium com- potassium, sodium. Therapeutic levels:
plex (MAC). Peak: life-threatening infections: 25–40
PRECAUTIONS mcg/mL; serious infections: 20–25 mcg/
mL; urinary tract infections: 15–20 mcg/
Contraindications: Hypersensitivity to mL. Trough: Less than 8 mcg/mL. Toxic
amikacin, other aminoglycosides. Cau- levels: Peak: greater than 40 mcg/mL;
tions: Preexisting renal impairment, trough: greater than 10 mcg/mL.
auditory or vestibular impairment, hy-
pocalcemia, elderly, pts with neuromus- AVAILABILITY (Rx)
cular disorder, dehydration, concomi- Injection Solution: 250 mg/mL.

underlined – top prescribed drug


amikacin 53
A
ADMINISTRATION/HANDLING Dosage in Renal Impairment
Dosage and frequency are modified based
IV on degree of renal impairment and serum
Reconstitution • Dilute to concentra- drug concentration. After a loading dose
tion of 0.25–5 mg/mL in 0.9% NaCl or D5W. of 5–7.5 mg/kg, maintenance dose and
Rate of administration • Infuse over frequency are based on serum creatinine
30–60 min. levels and creatinine clearance.
Storage • Store vials at room temper-
ature. • Solution appears clear but may Adults
become pale yellow (does not affect po- Creatinine Clearance Dosing Interval
tency). • Intermittent IV infusion (pig- 50 mL/min or greater No dose adjustment
gyback) is stable for 24 hrs at room 10–50 mL/min q24–72h
temperature, 2 days if refriger- Less than 10 mL/min q48–72h
ated. • Discard if precipitate forms or Hemodialysis q48–72h (give after
HD on ­dialysis
dark discoloration occurs. days)
IM Continuous renal Initially, 10 mg/kg,
replacement then 7.5 mg/kg
• To minimize discomfort, give deep IM ­therapy (CRRT) q24–48h
slowly. • Less painful if injected into
gluteus maximus rather than in lateral
Dosage in Hepatic Impairment
aspect of thigh.
No dose adjustment.
IV INCOMPATIBILITIES
Amphotericin, azithromycin (Zithro- SIDE EFFECTS
max), propofol (Diprivan). Frequent: Phlebitis, thrombophlebitis.
Occasional: Rash, fever, urticaria, pruri-
IV COMPATIBILITIES tus. Rare: Neuromuscular blockade (dif-
Amiodarone (Cordarone), aztreonam ficulty breathing, drowsiness, weakness).
(Azactam), calcium gluconate, cefepime
(Maxipime), cimetidine (Tagamet), cip- ADVERSE EFFECTS/TOXIC
rofloxacin (Cipro), clindamycin (Cleo- REACTIONS
cin), dexmedetomidine (Precedex), dil- Serious reactions include nephrotoxic-
tiaZEM (Cardizem), diphenhydrAMINE ity (increased thirst, decreased appetite,
(Benadryl), enalapril (Vasotec), esmolol nausea, vomiting, increased BUN and se-
(BreviBloc), fluconazole (Diflucan), fu- rum creatinine levels, decreased creati-
rosemide (Lasix), levoFLOXacin (Leva- nine clearance); neurotoxicity (muscle
quin), LORazepam (Ativan), magnesium twitching, visual disturbances, seizures,
sulfate, midazolam (Versed), morphine, paresthesia); ototoxicity (tinnitus, dizzi-
ondansetron (Zofran), potassium chlo- ness, loss of hearing).
ride, raNITIdine (Zantac), vancomycin.
NURSING CONSIDERATIONS
INDICATIONS/ROUTES/DOSAGE BASELINE ASSESSMENT
Usual Parenteral Dosage Obtain BUN, serum creatinine. Dehydration
Note: Individualization of dose is critical must be treated prior to aminoglycoside
due to low therapeutic index. Initial and therapy. Establish baseline hearing acuity
periodic peak and trough levels should before beginning therapy. Question for his-
be determined. tory of allergies, esp. to aminoglycosides
IV, IM: ADULTS, ELDERLY, CHILDREN, and sulfite. Obtain specimen for culture,
INFANTS: 5–7.5 mg/kg/dose q8h. NEO- sensitivity before giving first dose (therapy
NATES: 15 mg/kg/dose q12–48h (based may begin before results are known).
on weight).
Canadian trade name Non-Crushable Drug High Alert drug
54 amiodarone
A
INTERVENTION/EVALUATION USES
Monitor I&O (maintain hydration), Management of life-threatening recurrent
urinalysis. Monitor results of serum ventricular fibrillation, (VF) or recurrent he-
peak/trough levels. Be alert to ototoxic, modynamically unstable ventricular tachy-
neurotoxic, nephrotoxic symptoms (see cardia (VT) unresponsive to other therapy.
Adverse Effects/Toxic Reactions). Check OFF-LABEL: Treatment of atrial fibrillation,
IM injection site for pain, induration. paroxysmal supraventricular tachycardia
Evaluate IV site for phlebitis. Assess for (SVT); ventricular tachyarrhythmias.
skin rash, diarrhea, superinfection (par-
ticularly genital/anal pruritus), changes of PRECAUTIONS
oral mucosa. When treating pts with neu- Contraindications: Hypersensitivity to
romuscular disorders, assess respiratory amiodarone, iodine. Bradycardia-in-
response carefully. Therapeutic levels: duced syncope (except in the presence of
Peak: life-threatening infections: 25–40 a pacemaker), second- and third-degree
mcg/mL; serious infections: 20–25 mcg/ AV block (except in presence of a pace-
mL; urinary tract infections: 15–20 mcg/ maker); severe sinus node dysfunction,
mL. Trough: Less than 8 mcg/mL. Toxic causing marked sinus bradycardia; car-
levels: Peak: greater than 40 mcg/mL; diogenic shock. Cautions: May prolong
trough: greater than 10 mcg/mL. QT interval. Thyroid disease, electrolyte
imbalance, hepatic disease, hypotension,
PATIENT/FAMILY TEACHING
left ventricular dysfunction, pulmonary
• Continue antibiotic for full length of disease. Pts taking warfarin, surgical pts.
treatment. • Space doses evenly. • IM
injection may cause discomfort. • Re- ACTION
port any hearing, visual, balance, urinary Inhibits adrenergic stimulation; affects
problems, even after therapy is com- Na, K, Ca channels; prolongs action po-
pleted. • Do not take other medica- tential and refractory period in myocar-
tions without consulting physician. dial tissue. Decreases AV conduction and
sinus node function. Therapeutic Ef-
fect: Suppresses arrhythmias.
amiodarone PHARMACOKINETICS
a-mi-oh-da-rone Route Onset Peak Duration
(Cordarone , Nexterone, Pacerone) PO 3 days–3 1 wk–5 7–50 days
j BLACK BOX ALERT jPts should wks mos ­after discon-
be hospitalized when amiodarone is tinuation
initiated. Alternative therapies should
be tried first before using amiodar- Slowly, variably absorbed from GI tract.
one. Only indicated for pts with life- Protein binding: 96%. Extensively me-
threatening arrhythmias due to risk of tabolized in liver. Excreted via bile; not
toxicity. Pulmonary toxicity may occur
without symptoms. Hepatotoxicity removed by hemodialysis. Half-life:
is common, usually mild (rarely pos- 26–107 days; metabolite: 61 days.
sible). Can exacerbate arrhythmias.
Do not confuse amiodarone LIFESPAN CONSIDERATIONS
with aMILoride, dronedarone, Pregnancy/Lactation: Crosses placenta;
or Cordarone with Cardura. distributed in breast milk. May adversely
affect fetal development. Children: Safety
uCLASSIFICATION and efficacy not established. Elderly: May
PHARMACOTHERAPEUTIC: Cardiac be more sensitive to effects on thyroid func-
agent. CLINICAL: Antiarrhythmic. tion. May experience increased incidence of
Class III. ataxia, other neurotoxic effects.

underlined – top prescribed drug


amiodarone 55
A
INTERACTIONS hr, concentration not to exceed 2 mg/mL
DRUG: May increase QT interval–prolong- unless CVC used.
ing effect of citalopram, clarithromycin, Storage • Store at room tempera-
erythromycin, nilotinib, quetiapine, ture. • Stable for 24 hrs when diluted
ribociclib, thioridazine, voriconazole. in glass or polyolefin containers; stable
Fingolimod, levofloxacin may enhance for 2 hrs when diluted in PVC containers.
QT interval-prolonging effect. Beta block- PO
ers (e.g., atenolol, carvedilol, meto- • Give consistently with regard to meals
prolol), calcium channel blockers to reduce GI distress. • Tablets may be
(e.g., diltiaZEM, verapamil), digoxin, crushed. • Do not give with grapefruit
sofosbuvir may increase the bradycardic products.
effect. HERBAL: Herbals with hypoten-
sive properties (e.g., garlic, ginger, IV INCOMPATIBILITIES
ginkgo biloba) may increase concen- CeFAZolin (Ancef), heparin, sodium bi-
tration/effects. St. John’s wort may de- carbonate.
crease concentration/effect. May increase
concentration/effect of red yeast rice. IV COMPATIBILITIES
FOOD: Grapefruit products may alter Dexmedetomidine (Precedex), DOBU-
effect. Avoid use during therapy. LAB VAL- Tamine (Dobutrex), DOPamine (In-
UES: May increase serum ALT, AST, alkaline tropin), furosemide (Lasix), insulin
phosphatase, ANA titer. May cause changes (regular), labetalol (Normodyne), lido-
in ECG, thyroid function test results. Thera- caine, LORazepam (Ativan), midazolam
peutic serum level: 0.5–2.5 mcg/mL; (Versed), morphine, nitroglycerin, nor-
toxic serum level not established. epinephrine (Levophed), phenylephrine
(Neo-Synephrine), potassium chloride,
AVAILABILITY (Rx) vancomycin.
Infusion (Pre-Mix):Nexterone: 150 mg/100
mL; 360 mg/200 mL. Injection, Solu­ INDICATIONS/ROUTES/DOSAGE
tion: 50 mg/mL, 3 mL, 9 mL, 18 mL. Tablets: Ventricular Arrhythmias
(Pacerone): 100 mg, 200 mg, 400 mg. PO: ADULTS, ELDERLY: Initially, 400
mg q8–12h for 1–2 wks, then decrease
ADMINISTRATION/HANDLING to 200–400 mg once daily. Mainte-
nance: 200–400 mg/day.
IV
IV infusion: ADULTS, ELDERLY: Initially,
Reconstitution • Infusions longer 150 mg over 10 min, then 1 mg/min over
than 2 hrs must be administered/diluted 6 hrs; then 0.5 mg/min. Continue this
in glass or polyolefin bottles. • Dilute rate over at least 18 hrs or until complete
loading dose (150 mg) in 100 mL D5W transition or oral. Breakthrough stable
(1.5 mg/mL). • Dilute maintenance VT: 150 mg in 100 mL D5W or NS over
dose (900 mg) in 500 mL D5W (1.8 mg/ 10 min. 1–6 mg/mL.
mL). Concentrations greater than 3 mg/
Dosage in Renal Impairment
mL cause peripheral vein phlebitis.
Rate of administration • Does not
No dose adjustment.
need protection from light during admin- Dosage in Hepatic Impairment
istration. • Administer through central Use caution.
venous catheter (CVC) if possible, using
in-line filter. • Bolus over 10 min (15 SIDE EFFECTS
mg/min) not to exceed 30 mg/min; then Expected: Corneal microdeposits noted in
1 mg/min over 6 hrs; then 0.5 mg/min almost all pts treated for more than 6 mos
over 18 hrs. • Infusions longer than 1 (can lead to blurry vision). Occasional

Canadian trade name Non-Crushable Drug High Alert drug


56 amitriptyline
A
(greater than 3%): PO: Constipation, head- loss, difficulty breathing). Monitor se-
ache, decreased appetite, nausea, vomiting, rum ALT, AST, alkaline phosphatase for
paresthesia, photosensitivity, muscular in- evidence of hepatic toxicity. Assess skin,
coordination. Parenteral: Hypotension, cornea for bluish discoloration in pts who
nausea, fever, bradycardia. Rare (less than have been on drug therapy longer than 2
3%): PO: Bitter or metallic taste, decreased mos. Monitor thyroid function test results.
libido, dizziness, facial flushing, blue-gray If elevated hepatic enzymes occur, dosage
coloring of skin (face, arms, and neck), reduction or discontinuation is neces-
blurred vision, bradycardia, asymptomatic sary. Monitor for therapeutic serum level
corneal deposits, rash, visual disturbances, (0.5–2.5 mcg/mL). Toxic serum level not
halo vision. established.
ADVERSE EFFECTS/ PATIENT/FAMILY TEACHING
TOXIC REACTIONS • Protect against photosensitivity reaction
Serious, potentially fatal pulmonary on skin exposed to sunlight. • Bluish
toxicity (alveolitis, pulmonary fibrosis, skin discoloration gradually disappears
pneumonitis, acute respiratory distress when drug is discontinued. • Report
syndrome) may begin with progressive shortness of breath, cough. • Outpa-
dyspnea and cough with crackles, de- tients should monitor pulse before taking
creased breath sounds, pleurisy, HF, or medication. • Do not abruptly discon-
hepatotoxicity. May worsen existing ar- tinue medication. • Compliance with
rhythmias or produce new arrhythmias. therapy regimen is essential to control
­arrhythmias. • Restrict salt, alcohol
NURSING CONSIDERATIONS ­intake. • Avoid grapefruit prod-
ucts. • Recommend ophthalmic exams
BASELINE ASSESSMENT q6mos. • Report any vision changes,
Obtain baseline serum ALT, AST, alkaline signs/symptoms of cardiac arrhythmias.
phosphatase, ECG; pulmonary function
tests, CXR in pts with pulmonary disease.
Assess B/P, apical pulse immediately before
drug is administered (if pulse is 60/min or
less or systolic B/P is less than 90 mm Hg,
amitriptyline
withhold medication, contact physician). a-mi-trip-ti-leen
INTERVENTION/EVALUATION (Levate , Elavil)
Monitor for symptoms of pulmonary tox- j BLACK BOX ALERT jIncreased
icity (progressively worsening dyspnea, risk of suicidal thinking and behav-
ior in children, adolescents, young
cough). Dosage should be discontinued adults 18–24 yrs with major depres-
or reduced if toxicity occurs. Assess pulse sive disorder, other psychiatric
for quality, rhythm, bradycardia. Monitor disorders.
ECG for cardiac changes (e.g., widening of Do not confuse amitriptyline
QRS, prolongation of PR and QT intervals). with aminophylline, imipra-
Notify physician of any significant interval mine, or nortriptyline, or
changes. Assess for nausea, fatigue, pares- Elavil with Eldepryl, enalapril,
thesia, tremor. Monitor for signs of hypo- Equanil, or Mellaril.
thyroidism (periorbital edema, lethargy,
pudgy hands/feet, cool/pale skin, vertigo, FIXED-COMBINATION(S)
night cramps) and hyperthyroidism (hot/ Limbitrol: amitriptyline/chlordiaz-
dry skin, bulging eyes [exophthalmos], ePOXIDE (an antianxiety): 12.5 mg/5
frequent urination, eyelid edema, weight mg, 25 mg/10 mg.

underlined – top prescribed drug


amitriptyline 57
A
uCLASSIFICATION effects. Caution in pts with cardiovascular
PHARMACOTHERAPEUTIC: Tricyclic. disease.
CLINICAL: Antidepressant.
INTERACTIONS
DRUG: CNS depressants (e.g., al-
cohol, morphine, zolpidem) may
USES increase CNS depression. May increase
Treatment of unipolar, major depression. CNS depressant effect of azelastine.
OFF-LABEL: Neuropathic pain, related to Aclidinium, ipratropium, tiotro-
diabetic neuropathy or postherpetic neu- pium, umeclidinium may increase
ralgia; treatment of migraine. Treatment anticholinergic effect. May increase ar-
of depression in children, post-traumatic rhythmogenic effect of dronedarone.
stress disorder (PTSD). MAOIs (e.g., phenelzine, selegiline)
may increase the serotonergic effect.
PRECAUTIONS HERBAL: Herbals with sedative prop-
Contraindications: Hypersensitiv- erties (e.g., chamomile, kava kava,
ity to amitriptyline. Acute recovery valerian) may increase CNS depression.
period after MI, co-administered St. John’s wort may decrease concen-
with or within 14 days of MAOIs. Cau- tration/effects. FOOD: None known. LAB
tions: Prostatic hypertrophy, history of VALUES: May alter ECG ­ readings (flat-
urinary retention or obstruction, nar- tened T wave), serum glucose (increase
row-angle glaucoma, diabetes, seizures, or decrease). Therapeutic serum
hyperthyroidism, cardiac/hepatic/renal level: Peak: 120–250 ng/mL; toxic se-
disease, schizophrenia, xerostomia, vi- rum level: greater than 500 ng/mL.
sual problems, constipation or bowel
obstruction, elderly, increased intra- AVAILABILITY (Rx)
ocular pressure (IOP), hiatal hernia, Tablets:10 mg, 25 mg, 50 mg, 75 mg,
suicidal ideation. 100 mg, 150 mg.
ACTION ADMINISTRATION/HANDLING
Blocks reuptake of neurotransmitters PO
(norepinephrine, serotonin) at presyn- • Give with food or milk if GI distress
aptic membranes, increasing synaptic occurs.
concentration in the CNS. Therapeutic
Effect: Antidepressant effect. INDICATIONS/ROUTES/DOSAGE
Depression
PHARMACOKINETICS PO: ADULTS: Initially, 25–50 mg/day as
Rapidly and well absorbed from GI a single dose at bedtime, or in divided
tract. Protein binding: 90%. Metabo- doses. May gradually increase up to
lized in liver. Primarily excreted in urine. 100–300 mg/day. Titrate to lowest effec-
Minimal removal by hemodialysis. Half- tive dosage. ELDERLY: 10 mg 3 times/day
life: 10–26 hrs. and 20 mg at bedtime. ADOLESCENTS: 10
mg 3 times/day and 20 mg at bedtime.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses pla- Pain Management
centa; minimally distributed in breast PO: ADULTS, ELDERLY: 25–50 mg at bed-
milk. Children: More sensitive to in- time. May increase to 150 mg/day. CHIL-
creased dosage, toxicity, increased risk DREN: Initially, 0.1 mg/kg. May increase
of suicidal ideation, worsening of depres- over 2 wks to 0.5–2 mg/kg at bedtime.
sion. Elderly: Increased risk of toxicity. Dosage in Renal/Hepatic Impairment
Increased sensitivity to anticholinergic Use with caution.
Canadian trade name Non-Crushable Drug High Alert drug
58 amLODIPine
A
SIDE EFFECTS • Sensitivity to sun may occur. • Report
Frequent: Dizziness, drowsiness, dry visual disturbances. • Do not abruptly
mouth, orthostatic hypotension, headache, discontinue medication. • Avoid tasks
increased appetite, weight gain, nausea, that require alertness, motor skills until
unusual fatigue, unpleasant taste. Occa- response to drug is established. • Avoid
sional: Blurred vision, confusion, consti- alcohol. • Sips of water may relieve dry
pation, hallucinations, delayed micturition, mouth.
eye pain, arrhythmias, fine muscle tremors,
parkinsonian syndrome, anxiety, diar-
rhea, diaphoresis, heartburn, insomnia.
Rare: Hypersensitivity, alopecia, tinnitus, amLODIPine
breast enlargement, photosensitivity.
am-loe-di-peen
ADVERSE EFFECTS/TOXIC (Norvasc)
REACTIONS Do not confuse amLODIPine
Overdose may produce confusion, seizures, with aMILoride, or Norvasc with
severe drowsiness, changes in cardiac con- Navane or Vascor.
duction, fever, hallucinations, agitation,
dyspnea, vomiting, unusual fatigue, weak- FIXED-COMBINATION(S)
ness. Abrupt withdrawal after prolonged Amturnide: amLODIPine/aliskiren
therapy may produce headache, malaise, (a renin inhibitor)/hydroCHLOROthi-
nausea, vomiting, vivid dreams. Blood dys- azide (a diuretic): 5 mg/150 mg/12.5
crasias, cholestatic jaundice ­occur rarely. mg, 5 mg/300 mg/12.5 mg, 5 mg/300
mg/25 mg, 10 mg/300 mg/12.5 mg,
NURSING CONSIDERATIONS 10 mg/300 mg/25 mg. Azor: amLO-
DIPine/olmesartan (an angiotensin
BASELINE ASSESSMENT II receptor antagonist): 5 mg/20 mg,
Observe and record behavior. Assess psy- 10 mg/20 mg, 5 mg/40 mg, 10 mg/40
chological status, thought content, suicidal mg. Caduet: amLODIPine/atorv-
ideation, sleep patterns, appearance, inter- astatin (hydroxymethylglutaryl-CoA
est in environment. For pts on long-term [HMG-CoA] reductase inhibitor): 2.5
therapy, hepatic/renal function tests, blood mg/10 mg, 2.5 mg/20 mg, 2.5 mg/40
counts should be performed periodically. mg, 5 mg/10 mg, 10 mg/10 mg, 5
mg/20 mg, 10 mg/20 mg, 5 mg/40
INTERVENTION/EVALUATION mg, 10 mg/40 mg, 5 mg/80 mg, 10
Supervise suicidal-risk pt closely dur- mg/80 mg. Exforge: amLODIPine/
ing early therapy (as depression less- valsartan (an angiotensin II receptor
ens, energy level improves, increasing antagonist): 5 mg/160 mg, 10 mg/160
suicide potential). Assess appearance, mg, 5 mg/320 mg, 10 mg/320 mg. Ex-
behavior, speech pattern, level of inter- forge HCT: amLODIPine/valsartan/
est, mood. Monitor B/P for hypoten- hydroCHLOROthiazide (a diuretic): 5
sion, pulse, arrhythmias. Therapeutic mg/160 mg/12.5 mg, 5 mg/160 mg/25
serum level: Peak: 120–250 ng/mL; toxic mg, 10 mg/160 mg/12.5 mg, 10
serum level: greater than 500 ng/mL. mg/160 mg/25 mg, 10 mg/320 mg/25
PATIENT/FAMILY TEACHING
mg. Lotrel: amLODIPine/benazepril
(an angiotensin-converting enzyme
• Go slowly from lying to standing. • Tol- [ACE] inhibitor): 2.5 mg/10 mg, 5
erance to postural hypotension, sedative mg/10 mg, 5 mg/20 mg, 5 mg/40
and anticholinergic effects usually develops mg, 10 mg/20 mg, 10 mg/40 mg.
during early therapy. • Maximum thera- Prestalia: amLODIPine/perindopril
peutic effect may be noted in 2–4 wks. (an ACE inhibitor): 2.5 mg/3.5 mg;

underlined – top prescribed drug


amLODIPine 59
A
5 mg/7 mg; 10 mg/14 mg. Tekamlo: LIFESPAN CONSIDERATIONS
amLODIPine/aliskiren (a renin inhibi- Pregnancy/Lactation: Unknown if
tor): 5 mg/150 mg, 5 mg/300 mg, 10 drug crosses placenta or is distributed
mg/150 mg, 10 mg/300 mg. Triben- in breast milk. Children: Safety and ef-
zor: amLODIPine/olmesartan/hydro- ficacy not established. Elderly: Half-life
CHLOROthiazide: 5 mg/20 mg/12.5 may be increased, more sensitive to hy-
mg, 5 mg/40 mg/12.5 mg, 5 mg/40 potensive effects.
mg/25 mg, 10 mg/40 mg/12.5 mg,
10 mg/40 mg/25 mg. Twynsta: am- INTERACTIONS
LODIPine/telmisartan (an angioten- DRUG: Strong CYP3A4 inducers (e.g.,
sin II receptor antagonist): 5 mg/40 carbamazepine, phenytoin, rifampin)
mg, 5 mg/80 mg, 10 mg/40 mg, 10 may decrease concentration/effect. An-
mg/80 mg. tihepaciviral combination products
uCLASSIFICATION may increase concentration/effect. May
increase concentration/effect of fosphe-
PHARMACOTHERAPEUTIC: Calcium nytoin, lomitapide, phenytoin, sim-
channel blocker (dihydropyridine). vastatin. HERBAL: St. John’s wort may
CLINICAL: Antihypertensive, antian-
decrease concentration/effect. Yohimbe
ginal. may decrease antihypertensive effect.
FOOD: Grapefruit products may increase
USES concentration, hypotensive effects. LAB VAL-
UES: May increase hepatic enzyme levels.
Management of hypertension, coronary
artery disease (chronic stable angina, vaso- AVAILABILITY (Rx)
spastic [Prinzmetal’s or variant] angina). Tablets: 2.5 mg, 5 mg, 10 mg.
PRECAUTIONS
ADMINISTRATION/HANDLING
Contraindications: Hypersensitivity to am-
PO
LODIPine. Cautions: Hepatic impairment,
severe aortic stenosis, hypertrophic car- • May give without regard to food.
diomyopathy with outflow tract obstruction. INDICATIONS/ROUTES/DOSAGE
ACTION Hypertension
Inhibits calcium movement across cardiac PO: ADULTS: Initially, 5 mg/day as a single
and vascular smooth muscle cell mem- dose. May titrate every 7–14 days. Maxi-
branes during depolarization. Thera- mum: 10 mg/day. SMALL-FRAME, FRAGILE,
ELDERLY, ADDITION TO OTHER ANTIHYPER-
peutic Effect: Dilates coronary arteries,
TENSIVES: 2.5 mg/day as a single dose. May
peripheral arteries/arterioles. Decreases
total peripheral vascular resistance and titrate q7–14 days. Maximum: 10 mg/day.
CHILDREN 6–17 YRS: 2.5–5 mg/day.
B/P by vasodilation.
CAD
PHARMACOKINETICS PO: ADULTS: 5–10 mg/day as a single
Route Onset Peak Duration dose. ELDERLY, PTS WITH HEPATIC INSUF-
PO 0.5–1 hr N/A 24 hrs FICIENCY: 5 mg/day as a single dose.

Slowly absorbed from GI tract. Protein Dosage in Renal Impairment


binding: 95%–98%. Metabolized in liver. No dose adjustment.
Excreted primarily in urine. Not removed Dosage in Hepatic Impairment
by hemodialysis. Half-life: 30–50 hrs ADULTS, ELDERLY: Hypertension: Initially,
(increased in elderly, pts with hepatic 2.5 mg/day. Angina: Initially, 5 mg/day. Ti-
cirrhosis). trate slowly in pts with severe impairment.
Canadian trade name Non-Crushable Drug High Alert drug
60 amoxicillin
A
SIDE EFFECTS USES
Frequent (greater than 5%): Peripheral Treatment of susceptible infections due to
edema, headache, flushing. Occasional streptococci, E. coli, E. faecalis, P. mi­
(5%–1%): Dizziness, palpitations, nau- rabilis, H. influenzae, N. gonorrhoeae,
sea, unusual fatigue or weakness (as- including ear, nose, and throat; lower
thenia). Rare (less than 1%): Chest pain, respiratory tract; skin and skin structure;
bradycardia, orthostatic hypotension. UTIs; acute uncomplicated gonorrhea;
H. pylori. OFF-LABEL: Treatment of Lyme
ADVERSE EFFECTS/ disease and typhoid fever. Postexposure
TOXIC REACTIONS prophylaxis for anthrax exposure.
Overdose may produce excessive periph-
eral vasodilation, marked hypotension PRECAUTIONS
with reflex tachycardia, syncope. Contraindications: Serious hypersensi-
tivity to amoxicillin, other beta-lactams.
NURSING CONSIDERATIONS Cautions: History of allergies (esp. ceph-
BASELINE ASSESSMENT alosporins), infectious mononucleosis,
renal impairment, asthma.
Assess baseline renal/hepatic function
tests, B/P, apical pulse. ACTION
INTERVENTION/EVALUATION Inhibits bacterial cell wall synthesis by
Assess B/P (if systolic B/P is less than binding to PCN-binding proteins. Thera-
90 mm Hg, withhold medication, peutic Effect: Bactericidal in suscep-
contact physician). Assess for periph- tible microorganisms.
eral edema behind medial malleolus PHARMACOKINETICS
(sacral area in bedridden pts). Assess
skin for flushing. Question for head- Well absorbed from GI tract. Protein
ache, asthenia. binding: 20%. Partially metabolized in
liver. Primarily excreted in urine. Re-
PATIENT/FAMILY TEACHING moved by hemodialysis. Half-life: 1–
• Do not abruptly discontinue medica- 1.3 hrs (increased in renal impairment).
tion. • Compliance with therapy regi-
men is essential to control hyperten- LIFESPAN CONSIDERATIONS
sion. • Avoid tasks that require Pregnancy/Lactation: Crosses pla-
alertness, motor skills until response to centa, appears in cord blood, amniotic
drug is established. • Do not ingest fluid. Distributed in breast milk in low con-
grapefruit products. centrations. May lead to allergic sensiti-
zation, diarrhea, candidiasis, skin rash in
infant. Children: Immature renal func-
tion in neonate/young infant may delay
renal excretion. Elderly: Age-related
amoxicillin renal impairment may require dosage
adjustment.
a-mox-i-sil-in
(Novamoxin ) INTERACTIONS
Do not confuse amoxicillin with DRUG: Allopurinol may increase
amoxapine or Atarax. incidence of rash. Probenecid may
increase concentration, toxicity risk.
uCLASSIFICATION Tetracyclines may decrease thera-
PHARMACOTHERAPEUTIC: Penicillin. peutic effect. HERBAL: None significant.
CLINICAL: Antibiotic. FOOD: None known. LAB VALUES: May
increase serum ALT, AST, bilirubin,
underlined – top prescribed drug
amoxicillin 61
A
BUN, creatinine, LDH. May cause posi- mL/min: ADULTS: 250–500 mg q12h.
tive Coombs’ test. CHILDREN: 8–20 mg/kg/dose q12h. Cre-
atinine clearance less than 10 mL/
AVAILABILITY (Rx) min: ADULTS: 250–500 mg q24h. CHIL-
Capsules: 250 mg, 500 mg. Powder for DREN: 8–20 mg/kg/dose q24h.
Oral Suspension: 125 mg/5 mL, 200
mg/5 mL, 250 mg/5 mL, 400 mg/5 mL. Dosage in Hepatic Impairment
Tablets: 500 mg, 875 mg. Tablets (Chew- No dose adjustment.
able): 125 mg, 250 mg.
SIDE EFFECTS
ADMINISTRATION/HANDLING Frequent: GI disturbances (mild diar-
PO rhea, nausea, vomiting), headache, oral/
• Give without regard to food. • In- vaginal candidiasis. Occasional: Gener-
struct pt to chew/crush chewable tablets alized rash, urticaria.
thoroughly before swallowing. • Oral ADVERSE EFFECTS/
suspension dose may be mixed with TOXIC REACTIONS
formula, milk, fruit juice, water,
cold drink. • Give immediately after Antibiotic-associated colitis, other super-
mixing. • After reconstitution, oral infections (abdominal cramps, severe
suspension is stable for 14 days at ei- watery diarrhea, fever) may result from
ther room temperature or refrigerated. altered bacterial balance in GI tract. Se-
vere hypersensitivity reactions, including
INDICATIONS/ROUTES/DOSAGE anaphylaxis, acute interstitial nephritis,
Susceptible Infections occur rarely.
PO: ADULTS, ELDERLY, CHILDREN, ADOLES-
CENTS (40 KG OR MORE): Mild
to moder- NURSING CONSIDERATIONS
ate: 250–500 mg q8h or 500–875 mg BASELINE ASSESSMENT
q12h or 775 mg (Moxatag) once daily.
CHILDREN OLDER THAN 3 MOS, ADOLES-
Question for history of allergies (esp.
CENTS (LESS THAN 40 KG): 25–50 mg/kg/
penicillins, cephalosporins), renal im-
day in divided doses q8h. Maximum pairment.
single dose: 500 mg. CHILDREN 3 MOS INTERVENTION/EVALUATION
AND YOUNGER: 25–50 mg/kg/day in di- Promptly report rash, diarrhea (fever,
vided doses q8h. NEONATE: 20–30 mg/ abdominal pain, mucus and blood in
kg/day in divided doses q12h. Mild to stool may indicate antibiotic-associated
moderate lower respiratory tract: colitis). Be alert for superinfection: fever,
ADULTS, ELDERLY: 500 mg q8h or 875 mg vomiting, diarrhea, anal/genital pruri-
q12h. Severe as step-down therapy: tus, black “hairy” tongue, oral mucosal
ADULTS, ELDERLY: 500 mg q8h or 875 mg changes (ulceration, pain, erythema).
q12h. INFANT, CHILDREN, ADOLESCENTS: Monitor renal/hepatic function tests.
80–100 mg/kg/day in divided doses q8h.
Maximum: 500 mg/dose. PATIENT/FAMILY TEACHING
• Continue antibiotic for full length
Dosage in Renal Impairment
of treatment. • Space doses evenly.
b ALERT c Immediate-release 875-mg
• Take with meals if GI upset oc-
tablet or 775-mg extended-release tablet curs. • Thoroughly crush or chew the
should not be used in pts with creatinine chewable tablets before swallow-
clearance less than 30 mL/min. Dosage ing. • Report rash, diarrhea, other new
interval is modified based on creatinine symptoms.
clearance. Creatinine clearance 10–30

Canadian trade name Non-Crushable Drug High Alert drug


62 amoxicillin/clavulanate
A
PHARMACOKINETICS
amoxicillin/ Well absorbed from GI tract. Protein
clavulanate binding: 20%. Partially metabolized
in liver. Primarily excreted in urine.
a-mox-i-sil-in/klav-yoo-la-nate Removed by hemodialysis. Half-life:
(Amoxi-Clav , Augmentin, Aug- 1–1.3 hrs (increased in renal impair-
mentin ES 600, Clavulin ) ment).
Do not confuse Augmentin with LIFESPAN CONSIDERATIONS
amoxicillin or Azulfidine.
Pregnancy/Lactation: Crosses pla-
uCLASSIFICATION centa, appears in cord blood, amniotic
PHARMACOTHERAPEUTIC: Penicil- fluid. Distributed in breast milk in low
lin. CLINICAL: Antibiotic. concentrations. May lead to allergic
sensitization, diarrhea, candidiasis, skin
rash in infant. Children: Immature
USES renal function in neonate/young infant
Treatment of susceptible infections due may delay renal excretion. Elderly: Age-
to streptococci, E. coli, E. faecalis, related renal impairment may require
P. mirabilis, beta-lactamase produc- dosage adjustment.
ing H. influenzae, Klebsiella spp., M.
INTERACTIONS
catarrhalis, and S. aureus (not methi-
cillin-resistant Staphylococcus aureus DRUG: Allopurinol may increase inci-
[MRSA]), including lower respiratory, dence of rash. Probenecid may increase
skin and skin structure, UTIs, otitis me- concentration, toxicity risk. Tetracy-
dia, sinusitis. OFF-LABEL: Chronic anti- clines may decrease therapeutic effect.
microbial suppression of prosthetic joint HERBAL: None significant. FOOD: None
infection. known. LAB VALUES: May increase
serum ALT, AST. May cause positive
PRECAUTIONS Coombs’ test.
Contraindications: Hypersensitivity to AVAILABILITY (Rx)
amoxicillin, clavulanate, any penicillins;
Powder for Oral Suspension: (Amo-
history of cholestatic jaundice or hepatic
clan, Augmentin): 125 mg–31.25
impairment with amoxicillin/clavulanate
mg/5 mL, 200 mg–28.5 mg/5 mL, 250
therapy. Augmentin XR (additional): Se-
mg–62.5 mg/5 mL, 400 mg–57 mg/5
vere renal impairment (creatinine clear-
mL, 600 mg–42.9 mg/5 mL. Tablets:
ance less than 30 mL/min), hemodialysis
(Augmentin): 250 mg–125 mg, 500
pt. Cautions: History of allergies, esp.
mg–125 mg, 875 mg–125 mg. Tablets
cephalosporins; renal impairment, infec-
(Chewable): (Augmentin): 200 mg–
tious mononucleosis.
28.5 mg, 400 mg–57 mg.
ACTION Tablets (Extended-Release): 1,000
Amoxicillin inhibits bacterial cell wall mg–62.5 mg.
synthesis by binding to PCN-binding
ADMINISTRATION/HANDLING
proteins. Clavulanate inhibits bacterial
beta-lactamase protecting amoxicillin PO
from degradation. Therapeutic Ef- • Store tablets at room temperature.
fect: Amoxicillin is bactericidal in sus- • After reconstitution, oral suspension
ceptible microorganisms. Clavulanate is stable for 10 days but should be refrig-
protects amoxicillin from enzymatic deg- erated. • May mix dose of suspension
radation. with milk, formula, or juice and give

underlined – top prescribed drug


amphotericin B 63
A
immediately. • Give without regard to SIDE EFFECTS
meals. • Give with food to increase ab- Occasional (9%–4%): Diarrhea, loose
sorption, decrease stomach upset. • In- stools, nausea, skin rashes, urticaria. Rare
struct pt to chew/crush chewable tablets (less than 3%): Vomiting, vaginitis, ab-
thoroughly before swallowing. • Do not dominal discomfort, flatulence, headache.
break, crush, dissolve, or divide ex-
tended-release tablets. ADVERSE EFFECTS/
TOXIC REACTIONS
INDICATIONS/ROUTES/DOSAGE
Antibiotic-associated colitis, other superin-
Note: Dosage based on amoxicillin fections (abdominal cramps, severe watery
component. diarrhea, fever) may result from altered
Usual Adult Dosage bacterial balance in GI tract. Severe hyper-
250 mg q8h or
PO: ADULTS, ELDERLY: sensitivity reactions, including anaphylaxis,
500 mg q8–12h or 875 mg q12h or acute interstitial nephritis, occur rarely.
2,000 mg q12h. NURSING CONSIDERATIONS
Usual Pediatric Dosage BASELINE ASSESSMENT
PO: CHILDREN OLDER THAN 3 MOS, WEIGH-
Question for history of allergies, esp. peni-
ING 40 KG OR MORE: (Mild-Moderate): 500
cillins, cephalosporins, renal impairment.
mg q12h or 250 mg q8h. (Severe): 875
mg q12h or 500 mg q8h. (Extended-­ INTERVENTION/EVALUATION
Release): 2,000 mg q12h. WEIGHING Promptly report rash, diarrhea (fever, ab-
LESS THAN 40 KG: (Mild-Moderate): 25 mg/ dominal pain, mucus and blood in stool
kg/day in 2 divided doses or 20 mg/kg/ may indicate antibiotic-associated colitis).
day in 3 divided doses. (Severe): 45 mg/ Be alert for signs of superinfection, includ-
kg/day in 2 divided doses or 40 mg/ ing fever, vomiting, diarrhea, black “hairy”
kg/day in 3 divided doses. Maximum tongue, ulceration or changes of oral mu-
single dose: 500 mg. YOUNGER THAN 3 cosa, anal/genital pruritus. Monitor renal/
MOS: Amoxicillin 30 mg/kg/day divided hepatic tests with prolonged therapy.
q12h using 125 mg/5mL suspension only.
PATIENT/FAMILY TEACHING
Usual Neonate Dosage
• Continue antibiotic for full length of
PO: NEONATES, CHILDREN YOUNGER
treatment. • Space doses evenly. • Take
THAN 3 MOS: 30 mg/kg/day (using 125 with meals if GI upset occurs. • Thor-
mg/5 mL suspension) in divided doses oughly crush or chew the chewable tablets
q12h. before swallowing. • Notify physician if
Dosage in Renal Impairment rash, diarrhea, other new symptoms occur.
b ALERT c Do not use 875-mg tablet or
extended-release tablets for creatinine
clearance less than 30 mL/min. amphotericin B
Dosage and frequency are modified based
on creatinine clearance. Creatinine am-foe-ter-i-sin
clearance 10–30 mL/min: 250–500
(Abelcet, AmBisome, Fungizone )
mg q12h. Creatinine clearance less
than 10 mL/min: 250–500 mg q24h.
j BLACK BOX ALERT j (Nonli-
posomal) To be used primarily for
HD: 250–500 mg q24h, give dose during pts with progressive, potentially
and after dialysis. PD: 250 mg q12h. fatal fungal infection. Not to be
used for noninvasive forms of
Dosage in Hepatic Impairment fungal disease (oral thrush, vaginal
No dose adjustment (see Contraindica- candidiasis).
tions).
Canadian trade name Non-Crushable Drug High Alert drug
64 amphotericin B
A
uCLASSIFICATION children); Abelcet, 7.2 days; AmBisome,
PHARMACOTHERAPEUTIC: Polyene 100–153 hrs; Amphotec, 26–28 hrs.
antifungal. CLINICAL: Antifungal, an- LIFESPAN CONSIDERATIONS
tiprotozoal.
Pregnancy/Lactation: Crosses pla-
centa; unknown if distributed in breast
USES milk. Children: Safety and efficacy not
Abelcet: Treatment of invasive fungal established, but use the least amount for
infections refractory or intolerant to Fun- therapeutic regimen. Elderly: No age-
gizone. AmBisome: Empiric treatment related precautions noted.
of fungal infection in febrile neutrope- INTERACTIONS
nic pts. Aspergillus, Candida species,
DRUG: Foscarnet may increase neph-
Cryptococcus infections refractory to
rotoxic effect. May decrease therapeu-
Fungizone or pt with renal impairment
tic effect of Saccharomyces boulardii.
or toxicity with Fungizone. Treatment of
HERBAL: None significant. FOOD: None
cryptococcal meningitis in HIV-infected
known. LAB VALUES: May increase se-
pts. Treatment of visceral leishmaniasis.
rum ALT, AST, alkaline phosphatase, BUN,
Fungizone: Treatment of life-­threatening
creatinine. May decrease serum calcium,
fungal infections caused by susceptible
magnesium, potassium.
fungi, including Candida spp., Histo­
plasma, Cryptococcus, Aspergillus, AVAILABILITY (Rx)
Blastomyces. OFF-LABEL: Abelcet: Se- Injection, Powder for Reconstitution:
rious Candida infections. AmBisome: (AmBisome, Fungizone): 50 mg. In-
Treatment of systemic histoplasmosis jection, Suspension: (Abelcet): 5 mg/
infection. mL (20 mL).
PRECAUTIONS ADMINISTRATION/HANDLING
Contraindications:Hypersensitivity to IV
amphotericin B. Cautions: Concomitant
use with other nephrotoxic drugs; renal • Use strict aseptic technique; no bacte-
impairment. riostatic agent or preservative is present
in diluent.
ACTION
Reconstitution • Abelcet: Shake 20-
Generally fungistatic but may become mL (100-mg) vial gently until contents
fungicidal with high dosages or very are dissolved. Withdraw required dose
susceptible microorganisms. Binds to using 5-micron filter needle (supplied by
sterols in fungal cell membrane. Thera- manufacturer). • Dilute with D5W to
peutic Effect: Alters fungal cell mem- 1–2 mg/mL. • AmBisome: Reconsti-
brane permeability, allowing loss of tute each 50-mg vial with 12 mL Sterile
potassium, other cellular components, Water for Injection to provide concentra-
resulting in cell death. tion of 4 mg/mL. • Shake vial vigorously
PHARMACOKINETICS for 30 sec. Withdraw required dose and
inject syringe contents through a 5-micron
Protein binding: 90%. Widely distrib- filter into an infusion of D5W to provide
uted. Metabolism not specified. Cleared final concentration of 1–2 mg/mL (0.2–
by nonrenal pathways. Minimal removal 0.5 mg/mL for infants and small chil-
by hemodialysis. Amphotec and Abelcet dren). • Fungizone: Add 10 mL Ster-
are not dialyzable. Half-life: Fungi- ile Water for Injection to each 50-mg
zone, 24 hrs (increased in neonates and

underlined – top prescribed drug


amphotericin B 65
A
vial. • Further dilute with 250–500 mL Usual AmBisome Dose
D5W. • Final concentration should not IV infusion: ADULTS, CHILDREN: 3–6
exceed 0.1 mg/mL (0.25 mg/mL for cen- mg/kg/day over 2 hrs.
tral infusion).
Rate of administration • Give by Fungizone, Usual Dose
slow IV infusion. Infuse conventional IV infusion: ADULTS, ELDERLY: Dos-
amphotericin over 4–6 hrs; Abelcet over age based on pt tolerance and severity
2 hrs (shake contents if infusion longer of infection. Initially, 1-mg test dose
than 2 hrs); Amphotec over minimum of is given over 20–30 min. If tolerated,
2 hrs (avoid rate faster than 1 mg/kg/hr); usual dose is 0.3–1.5 mg/kg/day.
AmBisome over 1–2 hrs. Once therapy established, may give
Storage • Abelcet: Refrigerate unre- q48h at 1–1.5 mg/kg q48h. Maxi-
constituted solution. Reconstituted solu- mum: 1.5 mg/kg/day. CHILDREN: Test
tion is stable for 48 hrs if refrigerated, 6 dose of 0.1 mg/kg/dose (maxi-
hrs at room temperature. • AmBisome: mum: 1 mg) is infused over 30–60
Refrigerate unreconstituted solution. Re- min. If test dose is tolerated, usual
constituted vials are stable for 24 hrs when initial dose is 0.25–0.5 mg/kg/day.
refrigerated. Concentration of 1–2 mg/mL Gradually increase dose until desired
is stable for 6 hrs. • Fungizone: Refrig- dose achieved. Maximum: 1.5 mg/kg/
erate unused vials. • Once reconstituted, day. Once therapy is established, may
vials stable for 24 hrs at room tempera- give 1–1.5 mg/kg q48h. NEONATES:
ture, 7 days if refrigerated. • Diluted Initially, 1 mg/kg/dose once daily up
solutions stable for 24 hrs at room tem- to 1.5 mg/kg/day for short term. Once
perature, 2 days if refrigerated. therapy established, may give 1–1.5
mg/kg q48h.
IV INCOMPATIBILITIES
Note: Abelcet, AmBisome, Amphotec: Dosage in Renal/Hepatic Impairment
Do not mix with any other drug, diluent, No dose adjustment.
or solution. Fungizone: Allopurinol (Al-
oprim), aztreonam (Azactam), calcium
gluconate, cefepime (Maxipime), cimeti- SIDE EFFECTS
dine (Tagamet), ciprofloxacin (Cipro), Frequent (greater than 10%): Abelcet:
dexmedetomidine (Precedex), diphen- Chills, fever, increased serum cre-
hydrAMINE (Benadryl), DOPamine (In- atinine, multiple organ failure.
tropin), enalapril (Vasotec), filgrastim AmBisome: Hypokalemia, hypomag-
(Neupogen), fluconazole (Diflucan), nesemia, hyperglycemia, hypocalce-
foscarnet (Foscavir), magnesium sulfate, mia, edema, abdominal pain, back
meropenem (Merrem IV), ondansetron pain, chills, chest pain, hypotension,
(Zofran), piperacillin and tazobactam diarrhea, nausea, vomiting, headache,
(Zosyn), potassium chloride, propofol fever, rigors, insomnia, dyspnea, epi-
(Diprivan). staxis, increased hepatic/renal function
test results. Amphotec: Chills, fever,
IV COMPATIBILITIES hypotension, tachycardia, increased
LORazepam (Ativan). serum creatinine, hypokalemia, bili-
rubinemia. Amphocin: Fever, chills,
INDICATIONS/ROUTES/DOSAGE headache, anemia, hypokalemia, hypo-
Usual Abelcet Dose magnesemia, anorexia, malaise, gener-
IV infusion: ADULTS, CHILDREN: 3–5 mg/ alized pain, nephrotoxicity.
kg/day at rate of 2.5 mg/kg/hr.

Canadian trade name Non-Crushable Drug High Alert drug


66 ampicillin
A
ADVERSE EFFECTS/
TOXIC REACTIONS ampicillin
Cardiovascular toxicity (hypotension,
am-pi-sil-in
ventricular fibrillation), anaphylaxis
Do not confuse ampicillin with
occur rarely. Altered vision/hearing,
aminophylline.
seizures, hepatic failure, coagulation
defects, multiple organ failure, sepsis
­ uCLASSIFICATION
may occur. Each alternative formulation
PHARMACOTHERAPEUTIC: Penicillin.
is less nephrotoxic than conventional am-
CLINICAL: Antibiotic.
photericin (Amphocin).
NURSING CONSIDERATIONS USES
BASELINE ASSESSMENT Treatment of susceptible infections due
Obtain baseline BMP, LFT, serum mag- to streptococci, S. pneumoniae, staphy-
nesium, ionized calcium. Question for lococci (non–penicillinase-producing),
history of allergies, esp. to amphotericin meningococci, Listeria, some Klebsiella,
B, sulfite. Avoid, if possible, other neph- E. coli, H. influenzae, Salmonella, Shi­
rotoxic medications. Obtain premedi- gella, including GI, GU, respiratory infec-
cation orders (antipyretics, antihista- tions, meningitis, endocarditis prophy-
mines, antiemetics, corticosteroids) laxis. OFF-LABEL: Surgical prophylaxis
to reduce adverse reactions during IV for liver transplantation.
therapy.
PRECAUTIONS
INTERVENTION/EVALUATION Contraindications: Hypersensitivity to
Monitor B/P, temperature, pulse, res- ampicillin or any penicillin. Infections
pirations; assess for adverse reactions caused by penicillinase-producing or-
(fever, tremors, chills, anorexia, nau- ganisms. Cautions: History of allergies,
sea, vomiting, abdominal pain) q15min esp. cephalosporins, renal impairment,
twice, then q30min for 4 hrs of initial asthmatic pts, infectious mononucleosis.
infusion. If symptoms occur, slow infu-
sion, administer medication for symp- ACTION
tomatic relief. For severe reaction, stop Inhibits cell wall synthesis in suscep-
infusion and notify physician. Evaluate tible microorganisms by binding to
IV site for phlebitis. Monitor I&O, renal PCN binding protein. Therapeutic
function tests for nephrotoxicity. Moni- Effect: Bactericidal in susceptible mi-
tor CBC, BMP (esp. potassium), LFT, croorganisms.
serum magnesium.
PHARMACOKINETICS
PATIENT/FAMILY TEACHING
Moderately absorbed from GI tract.
• Prolonged therapy (wks or mos) is Protein binding: 15%–25%. Widely dis-
usually necessary. • Fever reaction tributed. Partially metabolized in liver.
may decrease with continued ther- Primarily excreted in urine. Removed by
apy. • Muscle weakness may be hemodialysis. Half-life: 1–1.5 hrs (in-
noted during therapy (due to hypoka- creased in renal impairment).
lemia).
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses placenta;
appears in cord blood, amniotic fluid.

underlined – top prescribed drug


ampicillin 67
A
Distributed in breast milk in low concen- IM
trations. May lead to allergic sensitization, • Reconstitute each vial with Sterile Water
diarrhea, candidiasis, skin rash in infant. for Injection or Bacteriostatic Water for
Children: Immature renal function in Injection (consult individual vial for spe-
neonates/young infants may delay renal ex- cific volume of diluent). • Stable for 1
cretion. Elderly: Age-related renal impair- hr. • Give deeply in large muscle mass.
ment may require dosage adjustment.
PO
INTERACTIONS • Oral suspension, after reconstitution, is
DRUG: Allopurinol may increase inci- stable for 7 days at room temperature, 14
dence of rash. Probenecid may increase days if refrigerated. • Shake oral suspen-
concentration, toxicity risk. Tetracy- sion well before using. • Give orally 1–2
clines may decrease therapeutic effect. hrs before meals for maximum absorption.
HERBAL: None significant. FOOD: None IV INCOMPATIBILITIES
known. LAB VALUES: May increase
serum ALT, AST. May cause positive DiltiaZEM (Cardizem), midazolam
Coombs’ test. (Versed), ondansetron (Zofran).

AVAILABILITY (Rx) IV COMPATIBILITIES


Capsules: 500 mg. Injection, Powder for
Calcium gluconate, cefepime (Maxip-
Reconstitution: 125 mg, 250 mg, 500 mg,
ime), dexmedetomidine (Precedex),
1 g, 2 g. Powder for Oral Suspension: 125 DOPamine (Intropin), famotidine
mg/5 mL, 250 mg/5 mL. (Pepcid), furosemide (Lasix), heparin,
HYDROmorphone (Dilaudid), insulin
ADMINISTRATION/HANDLING (regular), levoFLOXacin (Levaquin), lip-
ids, magnesium sulfate, morphine, mul-
IV tivitamins, potassium chloride, propofol
Reconstitution • For IV injection, (Diprivan).
dilute each vial with 5 mL Sterile Water INDICATIONS/ROUTES/DOSAGE
for Injection or 0.9% NaCl (10 mL for
1- and 2-g vials). Maximum concen- Usual Dosage
tration: 100 mg/mL for IV push. • For PO: ADULTS, ELDERLY: 250–500 mg
intermittent IV infusion (piggyback), q6h. CHILDREN: 50–100 mg/kg/day in di-
further dilute with 50–100 mL 0.9% vided doses q6h. Maximum: 2–4 g/day.
NaCl. Maximum concentration: 30 IV, IM: ADULTS, ELDERLY: 1–2 g q4–6h
mg/mL. or 50–250 mg/kg/day in divided doses.
Rate of administration • For IV in- Maximum: 12 g/day. CHILDREN: 25–
jection, give over 3–5 min (125–500 200 mg/kg/day in divided doses q6h.
mg) or over 10–15 min (1–2 g). For Maximum: 12 g/day. NEONATES: 50
intermittent IV infusion (piggyback), in- mg/kg/dose q6–12h.
fuse over 15–30 min. • Due to poten- Dosage in Renal Impairment
tial for hypersensitivity/anaphylaxis, start
Creatinine
initial dose at few drops per min, in-
Clearance Dosage
crease slowly to ordered rate; stay with pt
first 10–15 min, then check q10min. 10–50 mL/min Administer q6–12h
Storage • IV solution, diluted with Less than 10 mL/ Administer q12–24h
min
0.9% NaCl, is stable for 8 hrs at room Hemodialysis 1–2 g q12–24h
temperature or 2 days if refrigerated. • If Peritoneal dialysis 250 mg q12h
diluted with D5W, is stable for 2 hrs at Continuous renal 2g, then 1–2 g q6–8h
room temperature or 3 hrs if refriger- replacement
ated. • Discard if precipitate forms. therapy (CRRT)

Canadian trade name Non-Crushable Drug High Alert drug


68 ampicillin/sulbactam
A
Dosage in Hepatic Impairment
No dose adjustment. ampicillin/
SIDE EFFECTS sulbactam
Frequent: Pain at IM injection site,
GI disturbances (mild diarrhea, nau- amp-i-sil-in/sul-bak-tam
sea, vomiting), oral or vaginal candi- (Unasyn)
diasis. Occasional: Generalized rash, uCLASSIFICATION
urticaria, phlebitis, thrombophlebitis
(with IV administration), headache. PHARMACOTHERAPEUTIC: Penicil-
Rare: Dizziness, seizures (esp. with IV
lin. CLINICAL: Antibiotic.
therapy).
USES
ADVERSE EFFECTS/
TOXIC REACTIONS Treatment of susceptible infections,
including intra-abdominal, skin/skin
Antibiotic-associated colitis, other super-
structure, gynecologic infections, due to
infections (abdominal cramps, severe
beta-lactamase–producing organisms, in-
watery diarrhea, fever) may result from
cluding H. influenzae, E. coli, Klebsiella,
altered bacterial balance in GI tract. Se-
Acinetobacter, Enterobacter, S. aureus,
vere hypersensitivity reactions, including
and Bacteroides spp. OFF-­LABEL: Endo-
anaphylaxis, acute interstitial nephritis,
carditis, community-acquired pneumo-
occur rarely.
nia, surgical prophylaxis, pelvic inflam-
NURSING CONSIDERATIONS matory disease.
BASELINE ASSESSMENT PRECAUTIONS
Question for history of allergies, esp. Contraindications:Hypersensitivity to
penicillins, cephalosporins; renal im- ampicillin, any penicillins, or sulbac-
pairment. tam. Hx of cholestatic jaundice, hepatic
impairment associated with ampicillin/
INTERVENTION/EVALUATION sulbactam. Cautions: History of allergies,
Promptly report rash (although com- esp. cephalosporins; renal impairment;
mon with ampicillin, may indicate hy- infectious mononucleosis; ­asthmatic pts.
persensitivity) or diarrhea (fever, ab-
dominal pain, mucus and blood in stool ACTION
may indicate antibiotic-associated coli- Ampicillin inhibits bacterial cell wall
tis). Evaluate IV site for phlebitis. Check synthesis by binding to PCN-binding pro-
IM injection site for pain, induration. teins. Sulbactam inhibits bacterial beta-
Monitor I&O, urinalysis, renal function lactamase, protecting ampicillin from
tests. Be alert for superinfection: fever, degradation. Therapeutic Effect: Bac-
vomiting, diarrhea, anal/genital pruri- tericidal in susceptible microorganisms.
tus, oral mucosal changes (ulceration,
pain, erythema). PHARMACOKINETICS
PATIENT/FAMILY TEACHING
Protein binding: 28%–38%. Widely dis-
tributed. Partially metabolized in liver.
• Continue antibiotic for full length of Primarily excreted in urine. Removed by
treatment. • Space doses evenly. • More hemodialysis. Half-life: 1–1.3 hrs (in-
effective if taken 1 hr before or 2 hrs after creased in renal impairment).
food/beverages. • Discomfort may oc-
cur with IM injection. • Report rash, di- LIFESPAN CONSIDERATIONS
arrhea, or other new symptoms. Pregnancy/Lactation: Crosses pla-
centa; appears in cord blood, amniotic
underlined – top prescribed drug
ampicillin/sulbactam 69
A
fluid. Distributed in breast milk in low ampicillin/125 mg sulbactam/mL. • Give
concentrations. May lead to allergic deeply into large muscle mass within 1 hr
sensitization, diarrhea, candidiasis, skin after preparation.
rash in infant. Children: Safety and ef-
ficacy not established in pts younger than IV INCOMPATIBILITIES
1 yr. Elderly: Age-related renal impair- Amiodarone (Cordarone), diltiaZEM
ment may require dosage adjustment. (Cardizem), IDArubicin (Idamycin), on-
dansetron (Zofran).
INTERACTIONS
DRUG: Allopurinol may increase IV COMPATIBILITIES
incidence of rash. Probenecid may Famotidine (Pepcid), heparin, insulin
increase concentration, toxicity risk. (regular), morphine.
Tetracyclines may decrease thera-
peutic effect. HERBAL: None significant. INDICATIONS/ROUTES/DOSAGE
FOOD: None known. LAB VALUES: May Usual Dosage Range
increase serum ALT, AST, alkaline phos- IV, IM: ADULTS, ELDERLY, CHILDREN 13
phatase, LDH, creatinine. May cause YRS AND OLDER: 1.5–3 g q6h. Maxi-
positive Coombs’ test. mum: 12 g/day. IV: CHILDREN 12 YRS AND
YOUNGER: 100–200 mg ampicillin/kg/
AVAILABILITY (Rx) day in divided doses q6h. Maximum: 12
1.5
Injection, Powder for Reconstitution: g/day (Unasyn), 8 g/day (ampicillin).
g (ampicillin 1 g/sulbactam 0.5 g), 3 g NEONATES: 100 mg (ampicillin)/kg/day
(ampicillin 2 g/sulbactam 1 g). in divided doses q8–12h.
Dosage in Renal Impairment
ADMINISTRATION/HANDLING Dosage and frequency are modified
IV based on creatinine clearance and sever-
ity of infection.
Reconstitution • For IV injection, di-
Creatinine
lute with Sterile Water for Injection to
Clearance Dosage
provide concentration of 375 mg/
mL. • For intermittent IV infusion (pig- Greater than 30 mL/ No dose adjustment
min
gyback), further dilute with 50–100 mL 15–30 mL/min 1.5–3 g q12h
0.9% NaCl. 5–14 mL/min 1.5–3 g q24h
Rate of administration • For IV in- Hemodialysis 1.5–3 g q12–24h (af-
jection, give slowly over minimum of ter HD on dialysis
10–15 min. • For intermittent IV infu- days)
sion (piggyback), infuse over 15–30 Peritoneal dialysis 1.5–3 g q12–24h
min. • Due to potential for hypersensi- Continuous renal 3 g, then 1.5–3 g
tivity/anaphylaxis, start initial dose at few replacement ther- q6–12h
apy (CRRT)
drops per min, increase slowly to or-
dered rate; stay with pt first 10–15 min,
then check q10min. Dosage in Hepatic Impairment
Storage • IV solution, diluted with No dose adjustment.
0.9% NaCl, is stable for up to 72 hrs if
refrigerated (4 hrs if diluted with
SIDE EFFECTS
D5W). • Discard if precipitate forms. Frequent: Diarrhea, rash (most com-
mon), urticaria, pain at IM injection
IM site, thrombophlebitis with IV adminis-
• Reconstitute each 1.5-g vial with 3.2 tration, oral or vaginal candidiasis. Oc-
mL Sterile Water for Injection or lido- casional: Nausea, vomiting, headache,
caine to provide concentration of 250 mg malaise, urinary retention.
Canadian trade name Non-Crushable Drug High Alert drug
70 anastrozole
A
ADVERSE EFFECTS/TOXIC USES
REACTIONS Treatment of advanced breast cancer in
Antibiotic-associated colitis, other super- postmenopausal women who have devel-
infections (abdominal cramps; severe, oped progressive disease while receiv-
watery diarrhea; fever) may result from ing tamoxifen therapy. First-line therapy
altered bacterial balance in GI tract. Se- in advanced or metastatic breast cancer
vere hypersensitivity reactions, including in postmenopausal women. Adjuvant
anaphylaxis, acute interstitial nephritis, treatment in early hormone receptor–
blood dyscrasias may occur. High dosage positive breast cancer in postmenopausal
may produce seizures. women. OFF-LABEL: Treatment of recur-
rent or metastatic endometrial or uterine
NURSING CONSIDERATIONS cancers; treatment of ovarian cancer.
BASELINE ASSESSMENT PRECAUTIONS
Question for history of allergies, esp. peni- Contraindications: Hypersensitivity to
cillins, cephalosporins; renal impairment. anastrozole. Pregnancy, women who may
INTERVENTION/EVALUATION
become pregnant. Cautions: Preexisting
ischemic cardiac disease, osteopenia
Promptly report rash (although common (higher risk of developing osteoporosis),
with ampicillin, may indicate hypersensi- hyperlipidemia. May increase fall risk
tivity) or diarrhea (fever, abdominal pain, with fractures during therapy in pts with
mucus and blood in stool may indicate history of osteoporosis.
antibiotic-associated colitis). Evaluate
IV site for phlebitis. Check IM injection ACTION
site for pain, induration. Monitor I&O, Inhibits aromatase, preventing conver-
urinalysis, renal function tests. Be alert sion of androstenedione to estrone, and
for superinfection: fever, vomiting, diar- testosterone to estradiol. Therapeutic
rhea, anal/genital pruritus, oral mucosal Effect: Decreases tumor mass or delays
changes (ulceration, pain, erythema). tumor progression.
PATIENT/FAMILY TEACHING
PHARMACOKINETICS
• Take antibiotic for full length of treat-
ment. • Space doses evenly. • Discom- Well absorbed into systemic circula-
fort may occur with IM injection. tion (absorption not affected by food).
• Report rash, diarrhea, or other new Protein binding: 40%. Metabolized in
symptoms. liver. Eliminated by biliary system and,
to a lesser extent, kidneys. Mean half-
life: 50 hrs in postmenopausal women.
Steady-state plasma levels reached in ap-
anastrozole proximately 7 days.
LIFESPAN CONSIDERATIONS
an-as-troe-zole
(Arimidex) Pregnancy/Lactation: Crosses placenta;
Do not confuse anastrozole may cause fetal harm. Unknown if distrib-
with letrozole, or Arimidex with uted in breast milk. Children: Safety and
Imitrex. efficacy not established. Elderly: No age-
related precautions noted.
uCLASSIFICATION
INTERACTIONS
PHARMACOTHERAPEUTIC: Aromatase
inhibitor. CLINICAL: Antineoplastic DRUG: Estrogen therapies may re-
hormone. duce concentration/effects. Tamoxi-
fen may reduce plasma concentration.
underlined – top prescribed drug
anidulafungin 71
A
HERBAL: None significant. FOOD: None vomiting. Monitor for onset of diarrhea;
known. LAB VALUES: May elevate serum offer antidiarrheal medication.
GGT level in pts with liver metastases.
PATIENT/FAMILY TEACHING
May increase serum ALT, AST, alkaline
phosphatase, total cholesterol, LDL. • Notify physician if nausea, asthenia,
hot flashes become unmanageable.
AVAILABILITY (Rx)
Tablets: 1 mg.
ADMINISTRATION/HANDLING
anidulafungin
PO a-nid-ue-la-fun-jin
• Give without regard to food. (Eraxis)
INDICATIONS/ROUTES/DOSAGE uCLASSIFICATION
Breast Cancer (Advanced) PHARMACOTHERAPEUTIC: Echino-
PO: ADULTS, ELDERLY: 1 mg once daily candin. CLINICAL: Antifungal.
(continue until tumor progresses).
Breast Cancer (Early, Adjuvant) USES
PO: ADULTS, ELDERLY: 1 mg once daily.
Treatment of candidemia, other forms of
Dosage in Renal/Hepatic Impairment Candida infections (e.g., intra-abdominal
No dose adjustment. abscess, peritonitis), esophageal candidiasis.

SIDE EFFECTS PRECAUTIONS


Frequent (16%–8%): Asthenia, nau- Contraindications: Hypersensitivity to
sea, headache, hot flashes, back pain, anidulafungin, other echinocandins. Cau-
vomiting, cough, diarrhea. Occasional tions: Hepatic impairment.
(6%–4%): Constipation, abdominal pain,
anorexia, bone pain, pharyngitis, dizzi- ACTION
ness, rash, dry mouth, peripheral edema, Inhibits synthesis of the enzyme glucan
pelvic pain, depression, chest pain, par- (vital component of fungal cell forma-
esthesia. Rare (2%–1%): Weight gain, tion), preventing fungal cell wall forma-
diaphoresis. tion. Therapeutic Effect: Fungistatic.

ADVERSE EFFECTS/TOXIC PHARMACOKINETICS


REACTIONS Distributed in tissue. Moderately bound
Thrombophlebitis, anemia, leukopenia to albumin. Protein binding: 84%–99%.
occur rarely. Vaginal hemorrhage occurs Slow chemical degradation; 30% ex-
rarely (2%). creted in feces over 9 days. Not removed
by hemodialysis. Half-life: 40–50 hrs.
NURSING CONSIDERATIONS
LIFESPAN CONSIDERATIONS
BASELINE ASSESSMENT
Pregnancy/Lactation: May be embryo-
Obtain baseline bone mineral density, to- toxic. Crosses placental barrier. Unknown if
tal cholesterol, LDL, mammogram, clini- distributed in breast milk. Children: Safety
cal breast exam. and efficacy not established. Elderly: No
INTERVENTION/EVALUATION age-related precautions noted.
Monitor for asthenia, dizziness; assist with INTERACTIONS
ambulation if needed. Assess for head-
DRUG: May decrease effect of Saccha­
ache, pain. Offer antiemetic for nausea,
romyces boulardii. HERBAL: None
Canadian trade name Non-Crushable Drug High Alert drug
72 apalutamide
A
significant. FOOD: None known. LAB Esophageal Candidiasis
VALUES: May increase serum alkaline IV: ADULTS, ELDERLY: Give single 100-
phosphatase, amylase, ALT, AST, bilirubin, mg loading dose on day 1, followed by
calcium, creatinine, CPK, LDH, lipase. May 50 mg/day thereafter for a minimum of
decrease serum albumin, bicarbonate, 14 days and for at least 7 days following
magnesium, protein, potassium; Hgb, Hct, resolution of symptoms.
WBCs, neutrophils, platelet count. May Dosage in Renal/Hepatic Impairment
prolong prothrombin time (PT). No dose adjustment.
AVAILABILITY (Rx)
SIDE EFFECTS
Injection, Powder for Reconstitution: 50-
mg vial, 100-mg vial. Rare (3%–1%): Diarrhea, nausea, head-
ache, rigors, peripheral edema.
ADMINISTRATION/HANDLING
ADVERSE EFFECTS/
IV TOXIC REACTIONS
Reconstitution • Reconstitute each Hypokalemia occurs in 4% of pts. Hyper-
50-mg vial with 15 mL Sterile Water for sensitivity reaction characterized by facial
Injection (100 mg with 30 mL). Swirl, do flushing, hypotension, pruritus, urticaria,
not shake. • Further dilute 50 mg with rash occurs rarely. Hepatitis, elevated
50 mL D5W or 0.9% NaCl (100 mg with LFT, hepatic failure was reported.
100 mL, 200 mg with 200 mL).
Rate of administration • Do not ex- NURSING CONSIDERATIONS
ceed infusion rate of 1.1 mg/min. Not for
BASELINE ASSESSMENT
IV bolus injection.
Storage • Refrigerate unreconstituted Obtain baseline CBC, BMP, LFT. Obtain
vials. Reconstituted vials are stable for 24 specimens for fungal culture prior to
hrs at room temperature. Infusion solution therapy. Treatment may be instituted be-
is stable for 48 hrs at room temperature. fore results are known.
IV INCOMPATIBILITIES INTERVENTION/EVALUATION
Amphotericin B (Abelcet, AmBisome), er- Monitor for evidence of hepatic dysfunc-
tapenem (INVanz), sodium bicarbonate. tion, hypokalemia. Monitor daily pattern
of bowel activity, stool consistency. Assess
IV COMPATIBILITIES for rash, urticaria.
Dexamethasone (Decadron), famoti-
PATIENT/FAMILY TEACHING
dine (Pepcid), furosemide (Lasix), HY-
DROmorphone (Dilaudid), LORazepam • For esophageal candidiasis, maintain
(Ativan), methylPREDNISolone (SOLU), diligent oral hygiene.
morphine. Refer to IV Compatibility Chart
in front of book.
INDICATIONS/ROUTES/DOSAGE
apalutamide
b ALERT c Duration of treatment based ap-a-loot-a-mide
on pt’s clinical response. In general, (Erleada)
treatment is continued for at least 14 Do not confuse apalutamide
days after last positive culture. with bicalutamide, enzalu-
Candidemia, Other Candida Infections tamide, or niltamide.
IV: ADULTS, ELDERLY: Give single 200-mg uCLASSIFICATION
loading dose on day 1, followed by 100
mg/day thereafter for at least 14 days after PHARMACOTHERAPEUTIC: Anti-
last positive culture. androgen. CLINICAL: Antineoplastic.

underlined – top prescribed drug


apalutamide 73
A
USES ritonavir), strong CYP2C8 inhibitors
Treatment of non-metastatic castration- (e.g., gemfibrozil, trimethoprim),
resistant prostate cancer (NM-CRPC). P-gp inhibitors (e.g., amiodarone,
azithromycin, captopril, carvedilol,
PRECAUTIONS cyclosporine, felodipine, ticagre-
Contraindications: Hypersensitivity to lor) may increase concentration/
apalutamide. Use in women who are effect. Strong CYP3A4 inducers
pregnant or may become pregnant. (e.g., carbamazepine, phenytoin,
Cautions: History of cardiovascular rifampin) may decrease concentra-
disease (HF, ischemic heart disease), tion/effect. HERBAL: None significant.
hypothyroidism, conditions predispos- FOOD: None known. LAB VALUES:
ing to seizure activity (traumatic brain May decrease Hgb, Hct, leukocytes, lym-
injury, brain tumor, prior CVA, seizure phocytes, RBCs. May increase serum cho-
disorder). Pts at risk for fractures (fre- lesterol, glucose, potassium, triglycerides.
quent falls, osteoporosis, chronic corti-
AVAILABILITY (Rx)
costeroid therapy), hyperglycemia (e.g.,
diabetes, recent surgery, chronic use of Tablets: 60 mg.
corticosteroids).
ADMINISTRATION/HANDLING
ACTION PO
Binds directly to ligands of androgen • Give without regard to food. • Swallow
receptor, preventing androgen-­ receptor tablets whole; do not break, cut, crush,
translocation, DNA binding, and receptor- or divide.
mediated transcription. Therapeutic Ef-
fect: Decreases proliferation of tumor INDICATIONS/ROUTES/DOSAGE
cells, increases apoptosis, resulting in Non-Metastatic Castration-Resistant
decreased tumor volume. Prostate Cancer
PO: ADULTS, ELDERLY: 240 mg once daily
PHARMACOKINETICS
(in combination with a gonadotropin-re-
Rapidly absorbed and widely distributed. leasing hormone analog agonist or antag-
Metabolized in liver. Protein binding: onist [if not received orchiectomy]). Con-
96%. Peak plasma concentration: 2 hrs. tinue until disease progression or
Steady-state reached in 4 wks. Excreted unacceptable toxicity.
in urine (65%), feces (24%). Half-life:
3 days. Dose Modification
Based on Common Terminology Criteria
LIFESPAN CONSIDERATIONS for Adverse Effects (CTCAE).
Pregnancy/Lactation: Not indicated
in female population. Males with female Toxicities or Intolerable Side Effects
partners of reproductive potential must Any Grade 3 toxicity or intolerable
use effective contraception during treat- side effect: Withhold treatment until re-
ment and up to 3 mos after discontinua- solved to Grade 1 or less, then resume at
tion. May cause fetal harm if administered same dose. If applicable, may decrease
in pregnant females. May cause decreased dose to 180 mg or 120 mg once daily.
fertility in males. Children: Safety and Seizures: Permanently discontinue.
efficacy not established. Elderly: No age- Dosage in Renal/Hepatic Impairment
related precautions noted. Mild to moderate impairment: No
INTERACTIONS dose adjustment. Severe impairment:
ESRD: Not specified; use caution.
DRUG: Strong CYP3A4 inhibitors
(e.g., clarithromycin, ­ketoconazole,
Canadian trade name Non-Crushable Drug High Alert drug
74 apixaban
A
SIDE EFFECTS i­ndicate low thyroid levels. • Immedi-
Frequent (39%–16%): Fatigue, asthenia, ately report symptoms of seizure activity
hypertension, rash, urticaria, conjunc- (confusion, convulsions, loss of con-
tivitis, stomatitis, diarrhea, nausea, ar- sciousness). • Report symptoms of ele-
thralgia, decreased weight. Occasional vated blood sugar levels (blurred vision,
(14%–6%): Hot flush, decreased appe- headache, increased thirst, frequent uri-
tite, early satiety, hypophagia, peripheral nation). • Do not take newly prescribed
edema, penile/scrotal edema, pruritus. medications unless approved by the pre-
scriber who originally started treatment.
ADVERSE EFFECTS/TOXIC
REACTIONS
Anemia, leukopenia, lymphopenia are apixaban
expected responses to therapy. Increased
incidence of falls (16% of pts) and frac- a-pix-a-ban
tures (12% of pts) was reported. Seizures (Eliquis)
reported in less than 1% of pts. Hypothy- j BLACK BOX ALERT jDiscon-
roidism reported in 8% of pts. Higher in- tinuation in absence of alternative
cidence of ischemic heart disease (4% of anticoagulation increases risk
pts), HF (2% of pts) has occurred. for thrombotic events. Spinal or
epidural hematoma resulting in
NURSING CONSIDERATIONS paralysis may occur with ­neuraxial
anesthesia or spinal/epidural
BASELINE ASSESSMENT ­puncture.
Do not confuse apixaban with
Obtain baseline CBC, BMP, TSH; B/P.
rivaroxaban, argatroban, or
Question history of cardiovascular dis-
dabigatran.
ease (HF, ischemic heart disease), hy-
pothyroidism, seizure disorder. Assess uCLASSIFICATION
risk for falls and fractures. Receive full
PHARMACOTHERAPEUTIC: Factor Xa
medication history and screen for inter-
inhibitor. CLINICAL: Anticoagulant.
actions. Offer emotional support.
INTERVENTION/EVALUATION
Monitor CBC, BMP, TSH; B/P periodically. USES
Monitor for symptoms of hypothyroidism Reduces risk for stroke, systemic embo-
(bradycardia, constipation, depression, lism in pts with nonvalvular atrial fibril-
fatigue, muscle weakness, weight gain), lation. Prophylaxis of DVT following hip
hyperglycemia, seizure activity. Assess or knee replacement surgery. Treatment
skin for rash. Question for any incidence of DVT and PE. Reduces risk of recur-
of falls, suspected fractures. rent DVT/PE following initial therapy.
OFF-LABEL: Prevention of recurrent
PATIENT/FAMILY TEACHING stroke or TIA.
• Sexually active men must wear con- PRECAUTIONS
doms with sexual activity during treatment
and for at least 3 mos after last dose. Contraindications: Severe hypersensitiv-
• Women who are pregnant or who plan ity to apixaban. Active pathologic bleed-
on becoming pregnant should not handle ing. Cautions: Mild to moderate hepatic
medication. • Treatment may increase impairment, severe renal impairment
risk of falls and fractures. Go slowly from (may increase bleeding risk). Avoid use
lying to standing. Use caution during in pts with severe hepatic impairment,
strenuous activity. • Slow heart rate, prosthetic heart valve, significant rheu-
constipation, depression, fatigue may matic heart disease.

underlined – top prescribed drug


apixaban 75
A
ACTION INDICATIONS/ROUTES/DOSAGE
Selectively, directly, and reversibly inhibits Nonvalvular Atrial Fibrillation
free and clot-bound factor Xa, a key factor PO: ADULTS, ELDERLY: 5 mg twice daily. In
in the intrinsic and extrinsic pathway of pts with at least 2 of the following charac-
blood coagulation cascade. Therapeutic teristics: age 80 yrs or older, body weight
Effect: Inhibits clot-induced platelet ag- 60 kg or less, serum creatinine 1.5 mg/dL
gregation, fibrin clot formation. or greater, concurrent use with CYP3A4, or
P-gp inhibitors (e.g., ketoconazole, ritona-
PHARMACOKINETICS vir), reduce dose to 2.5 mg twice daily.
Readily absorbed after PO administra-
tion. Peak plasma concentration: 3–4 DVT/PE Treatment
hrs. Protein binding: 87%. Metabolized PO: ADULTS, ELDERLY: 10 mg twice daily
in liver. Excreted primarily in urine, fe- for 7 days, then 5 mg twice daily.
ces. Half-life: 12 hrs.
DVT Prophylaxis (Hip/Knee Replacement)
LIFESPAN CONSIDERATIONS Note: Begin 12–24 hrs postoperatively.
Pregnancy/Lactation: Unknown if dis- ADULTS, ELDERLY: 2.5 mg twice daily
tributed in breast milk. Children: Safety (35 days for hip; 12 days for knee).
and efficacy not established. Elderly: No DVT Prophylaxis, Reduce Risk Recurrent
age-related precautions noted. DVT/PE
INTERACTIONS PO: ADULTS, ELDERLY: 2.5 mg twice daily
DRUG: CYP3A4 inducers (e.g., carBA- (after at least 6 mos of treatment).
Mazepine, rifAMPin) may decrease level/ Dosage in Renal Impairment
effect. Anticoagulants (e.g., dabigatran, DVT/PE/Reduce risk recurrent DVT,
heparin, warfarin), antiplatelets (e.g., postoperative: No adjustment. Non-
aspirin, clopidogrel), NSAIDs (e.g., valvular A-fib, HD: SCR LESS THAN
diclofenac, ibuprofen, naproxen), 1.5: No adjustment. SCR 1.5 OR GREATER,
CYP3A4 inhibitors, (e.g., ketocon- OLDER THAN 80 YRS, WEIGHING 60 KG OR
azole, clarithromycin) may increase LESS: 2.5 mg 2 times/day.
concentration, bleeding risk. HERBAL: St.
John’s wort may decrease concentra- Dosage in Hepatic Impairment
tion/effect. Herbals with anticoagulant/ Mild impairment: No dose adjustment.
antiplatelet properties (e.g., garlic, Moderate impairment: Use caution.
ginger, ginkgo biloba) may increase risk Severe impairment: Not recommended.
of bleeding. FOOD: Grapefruit products
may increase level/adverse effects. LAB VAL- SIDE EFFECTS
UES: May decrease platelet count, Hgb, LFT. Rare (3%–1%): Nausea, ecchymosis.
AVAILABILITY (Rx) ADVERSE EFFECTS/­
Tablets: 2.5 mg, 5 mg. TOXIC REACTIONS
ADMINISTRATION/HANDLING Increased risk for bleeding/hemorrhagic
events. May cause serious, potentially fatal
b ALERT c Discontinuation in absence
bleeding, accompanied by one or more of
of alternative anticoagulation increases the following: a decrease in Hgb of 2 g/
risk for thrombotic events. dL or more; a need for 2 or more units of
PO
packed RBCs; bleeding occurring at one of
• Give without regard to food. • If the following sites: intracranial, intraspinal,
elective surgery or invasive procedures intraocular, pericardial, intra-articular, in-
with moderate or high risk for bleeding, tramuscular with compartment syndrome,
discontinue apixaban at least 24–48 hrs retroperitoneal. Serious reactions include
prior to procedure.
Canadian trade name Non-Crushable Drug High Alert drug
76 apremilast
A
jaundice, cholestasis, cytolytic hepatitis, USES
Stevens-Johnson syndrome, hypersensitiv- Treatment of adult pts with active psori-
ity reaction, anaphylaxis. atic arthritis, moderate to severe plaque
psoriasis who are candidates for photo-
NURSING CONSIDERATIONS
therapy or systemic therapy.
BASELINE ASSESSMENT
PRECAUTIONS
Obtain baseline CBC. Question history of
bleeding disorders, recent surgery, spi- Contraindications: Hypersensitivity to
nal punctures, intracranial hemorrhage, apremilast. Cautions: History of depres-
bleeding ulcers, open wounds, anemia, sion, severe renal impairment, suicidal
hepatic impairment. Obtain full medica- ideation. Pts with latent infections (e.g.,
tion history including herbal products. TB, viral hepatitis).

INTERVENTION/EVALUATION ACTION
Periodically monitor CBC, stool for occult Selectively inhibits PDE4, increasing cyclic
blood. Be alert for complaints of abdomi- AMP (cAMP) and regulation of inflamma-
nal/back pain, headache, confusion, weak- tory mediators. Therapeutic Effect: Re-
ness, vision change (may indicate hemor- duces psoriatic arthritis exacerbations.
rhage). Question for increased menstrual PHARMACOKINETICS
bleeding/discharge. Assess for any sign of
bleeding: bleeding at surgical site, hema- Readily absorbed after PO administra-
turia, blood in stool, bleeding from gums, tion. Protein binding: 68%. Peak plasma
petechiae, ecchymosis. concentration: 2.5 hrs. Metabolized in
liver. Excreted in urine (58%), feces
PATIENT/FAMILY TEACHING (39%). Half-life: 6–9 hrs.
• Do not take/discontinue any medica-
tion except on advice from physi-
LIFESPAN CONSIDERATIONS
cian. • Avoid alcohol, aspirin, NSAIDs, Pregnancy/Lactation: Unknown
herbal supplements, grapefruit prod- if distributed in breast milk. Not rec-
ucts. • Consult physician before surgery, ommended for nursing mothers.
dental work. • Use electric razor, soft Children: Safety and efficacy not es-
toothbrush to prevent bleeding. • Re- tablished. Elderly: No age-related pre-
port blood-tinged mucus from coughing, cautions noted.
heavy menstrual bleeding, headache, vi-
sion problems, weakness, abdominal
INTERACTIONS
pain, frequent bruising, bloody urine or DRUG: Strong CYP450 inducers
stool, joint pain or swelling. (e.g., carBAMazepine, PHENobar-
bital, phenytoin, rifAMPin) may
decrease concentration/effect. HERBAL:
St. John’s wort may decrease concen-
apremilast tration/effect. FOOD: None significant.
LAB VALUES: None known.
a-pre-mi-last
(Otezla) AVAILABILITY (Rx)
Do not confuse apremilast with
roflumilast. Tablets: 10 mg, 20 mg, 30 mg.

uCLASSIFICATION ADMINISTRATION/HANDLING
PHARMACOTHERAPEUTIC: Phospho- PO
diesterase 4 (PDE4) enzyme inhibitor. • Give without regard to food. Adminis-
CLINICAL: Antipsoriatic arthritis agent. ter whole; do not crush, cut, dissolve, or
divide.
underlined – top prescribed drug
aprepitant/fosaprepitant 77
A
INDICATIONS/ROUTES/DOSAGE b­ehavior. Report weight loss of any
Psoriatic Arthritis, Plaque Psoriasis kind. • Increase fluid intake if dehy-
PO: ADULTS/ELDERLY: Initially, titrate dration suspected. • Immediately notify
dose from day 1–day 5. Day 1: 10 mg in physician if pregnancy suspected. • Do
am only. Day 2: 10 mg in am; 10 mg in pm. not chew, crush, dissolve, or divide tablets.
Day 3: 10 mg in am; 20 mg in pm. Day
4: 20 mg in am; 20 mg in pm. Day 5: 20
mg in am; 30 mg in pm. Day 6/mainte- aprepitant/
nance: 30 mg twice daily.
fosaprepitant
Dosage in Renal Impairment (Creatinine
Clearance less than 30 mL/min) a-prep-i-tant/fos-a-prep-i-tant
Days 1–3: 10 mg in am. Days 4–5: 20 (Cinvanti, Emend)
mg in am, using only am schedule. Day 6/ Do not confuse fosaprepitant
maintenance: 30 mg once daily. with aprepitant, fosamprenavir,
or fospropofol.
Dosage in Hepatic Impairment
No dose adjustment. uCLASSIFICATION
PHARMACOTHERAPEUTIC: Neuro-
SIDE EFFECTS kinin receptor antagonist. CLINI-
Occasional (9%–4%): Nausea, diarrhea, CAL: Antinausea, antiemetic.
headache, upper respiratory tract infec-
tion. Rare (3% or less): Vomiting, naso-
pharyngitis, upper abdominal pain. USES
PO/IV: Prevention of nausea, vomit-
ADVERSE EFFECTS/TOXIC ing associated with repeat courses of
REACTIONS moderately to highly emetogenic cancer
Increased risk of depression reported in chemotherapy. PO: Prevention of postop
less than 1% of pts. Weight decrease of 5%– nausea, vomiting.
10% of body weight occurred in 10% of pts.
PRECAUTIONS
NURSING CONSIDERATIONS Contraindications: Hypersensitivity to
BASELINE ASSESSMENT
aprepitant or fosaprepitant. Concurrent
use with pimozide. Cautions: Severe
Obtain baseline weight, vital signs. Ques- hepatic impairment. Concurrent use of
tion history of depression, severe renal medications metabolized through CYP3A4
impairment, suicidal ideations. Screen (e.g., docetaxel, etoposide, ifosfamide,
for prior allergic reactions to drug class. imatinib, irinotecan, PACLitaxel, vinblas-
Receive full medication history including tine, vinCRIStine, vinorelbine).
herbal products. Assess degree of joint
pain, range of motion, mobility. ACTION
INTERVENTION/EVALUATION Inhibits substance P receptor, augments
Be alert for worsening depression, sui- antiemetic activity of 5-HT3 receptor an-
cidal ideation. Monitor for weight loss. tagonists. Therapeutic Effect: Prevents
Assess for dehydration if diarrhea occurs. acute and delayed phases of chemother-
Assess improvement of joint pain, range apy-induced emesis.
of motion, mobility. PHARMACOKINETICS
PATIENT/FAMILY TEACHING Moderately absorbed from GI tract.
• Report changes in mood or behav- Crosses blood-brain barrier. Extensively
ior, thoughts of suicide, self-destructive metabolized in liver. Protein binding:

Canadian trade name Non-Crushable Drug High Alert drug


78 aprepitant/fosaprepitant
A
greater than 95%. Eliminated primarily Rate of administration • Infuse over
by liver metabolism (not excreted re- 20–30 min 30 min prior to chemotherapy.
nally). Half-life: 9–13 hrs. Storage • Refrigerate unreconstituted
vials. • After reconstitution, solution is
LIFESPAN CONSIDERATIONS stable at room temperature for 24 hrs.
Pregnancy/Lactation: Unknown if IV Emulsion (Cinvanti)
drug crosses placenta or is distributed Reconstitution • For 130-mg dose, dilute
in breast milk. Children: Safety and ef- 18 mL of Cinvanti into 100 mL 0.9% NaCl or
ficacy not established. Elderly: No age- D5W infusion bag. • For 100-mg dose, di-
related precautions noted. lute 14 mL of Cinvanti into 100 mL 0.9%
NaCl or D5W infusion bag. • Mix by gentle
INTERACTIONS inversion (4–5 times). • Do not shake.
DRUG: Strong CYP3A4 inhibitors Rate of administration • Infuse over
(e.g., ketoconazole, clarithromy- 30 minutes. Use only non-DEHP tubing for
cin) may increase concentration/effect. administration. For IV injection, no further
Strong CYP3A4 inducers (e.g., car- dilution is necessary. Inject over 2 min.
BAMazepine, rifAMPin) may decrease
concentration/effect. May decrease effec- IV INCOMPATIBILITIES
tiveness of hormonal contraceptives, Do not infuse with any solutions contain-
warfarin. May increase concentration/ ing calcium or magnesium.
effect of bosutinib, budesonide, com-
bimetinib, neratinib, simeprevir. INDICATIONS/ROUTES/DOSAGE
HERBAL: St. John’s wort may decrease Prevention of Chemotherapy-Induced
concentration/effect. FOOD: Grapefruit Nausea, Vomiting
products may increase concentration/ Note: Administer in combination with
effect. LAB VALUES: May increase serum a 5-HT3 antagonist on day 1 and dexa-
ALT, AST, alkaline phosphatase, BUN, cre- methasone on days 1 through 4.
atinine, glucose. May produce proteinuria. PO: ADULTS, ELDERLY, CHILDREN 12 YRS OR
YOUNGER WEIGHING 30 KG OR MORE: 125
AVAILABILITY (Rx) mg 1 hr before chemotherapy on day 1
Capsules: (Emend): 40 mg, 80 mg, 125 and 80 mg once daily in the morning on
mg. Injection, Emulsion: (Cinvanti): 130 days 2 and 3.
mg/18 mL. Injection, Powder for Recon- IV: ADULTS, ELDERLY (SINGLE-DOSE REGI-
stitution: (Fosaprepitant): 150 mg. MEN): (Emend): 150 mg over 20–30
Suspension, Oral: 125 mg. min 30 min before to chemotherapy.
(Cinvanti): 100–130 mg over 30 min or
ADMINISTRATION/HANDLING IV injection over 2 min approx. 30 min
PO before chemotherapy.
• Give without regard to food. • Admin- Prevention of Postop Nausea, Vomiting
ister whole; do not cut, crush, or open PO: ADULTS, ELDERLY: 40 mg once within
capsules. • Suspension (prepared by 3 hrs prior to induction of anesthesia.
healthcare provider in oral dispenser).
Dispense in pt’s mouth along inner cheek. Dosage in Renal/Hepatic Impairment
Suspension is stable for 72 hrs if refriger- No dose adjustment. Caution in severe
ated or up 3 hrs at room temperature. hepatic impairment.
IV (Emend) SIDE EFFECTS
Reconstitution • Reconstitute each Frequent (17%–10%): Fatigue, nausea, hic-
vial with 5 mL 0.9% NaCl. • Add to 145 cups, diarrhea, constipation, anorexia.
mL 0.9% NaCl to provide a final concen- Occasional (8%–4%): Headache, vomiting,
tration of 1 mg/mL. dizziness, dehydration, heartburn. Rare
underlined – top prescribed drug
argatroban 79
A
(3% or less): Abdominal pain, epigastric PRECAUTIONS
discomfort, gastritis, tinnitus, insomnia. Contraindications: Hypersensitivity to
argatroban, active major bleeding. Cau-
ADVERSE EFFECTS/
tions: Severe hypertension, immediately
TOXIC REACTIONS
following lumbar puncture, spinal anes-
Neutropenia, mucous membrane disor- thesia, major surgery, pts with congenital
ders occur rarely. or acquired bleeding disorders, gastroin-
testinal ulcerations, hepatic impairment,
NURSING CONSIDERATIONS
critically ill pts.
BASELINE ASSESSMENT
Assess for dehydration (poor skin turgor,
ACTION
dry mucous membranes, longitudinal Direct thrombin inhibitor that reversibly
furrows in tongue). binds to thrombin-active sites of free
and clot-associated thrombin. Inhibits
INTERVENTION/EVALUATION thrombin-catalyzed or thrombin-induced
Monitor hydration, nutritional status, I&O. reactions, including fibrin formation, ac-
Assess bowel sounds for peristalsis. Assist tivation of coagulant factors V, VIII, and
with ambulation if dizziness occurs. Pro- XIII; inhibits protein C formation, platelet
vide supportive measures. Monitor daily aggregation. Therapeutic Effect: Pro-
pattern of bowel activity, stool consistency. duces anticoagulation.
PATIENT/FAMILY TEACHING PHARMACOKINETICS
• Relief from nausea/vomiting generally Distributed primarily in extracellular
occurs shortly after drug administra- fluid. Protein binding: 54%. Metabolized
tion. • Report persistent vomiting, in liver. Primarily excreted in the feces,
headache. • May decrease effectiveness presumably through biliary secretion.
of oral contraceptives. Half-life: 39–51 min (prolonged in
hepatic failure).
LIFESPAN CONSIDERATIONS
argatroban Pregnancy/Lactation: Unknown if ex-
ar-gat-roe-ban creted in breast milk. Children: Safety
Do not confuse argatroban with and efficacy not established. Elderly: No
Aggrastat. age-related precautions noted.
INTERACTIONS
uCLASSIFICATION
DRUG: Anticoagulants (e.g., dabi-
PHARMACOTHERAPEUTIC: Direct
gatran, heparin, rivaroxaban,
thrombin inhibitor. CLINICAL: Anti- warfarin), antiplatelets (e.g., as-
coagulant. pirin, clopidogrel), NSAIDs (e.g.,
diclofenac, ibuprofen, naproxen)
USES may increase anticoagulant effect.
HERBAL: Herbals with anticoagu-
Prophylaxis or treatment of thrombosis lant/antiplatelet properties (e.g.,
in heparin-induced thrombocytopenia garlic, ginger, ginkgo biloba) may
(HIT) in pts with HIT or at risk of de- increase risk of bleeding. FOOD: None
veloping HIT undergoing percutaneous known. LAB VALUES: Prolongs pro-
coronary procedures. OFF-LABEL: Main- thrombin time (PT), activated partial
tain extracorporeal circuit patency of thromboplastin time (aPTT), inter-
continuous renal replacement therapy national normalized ratio (INR). May
(CRRT) in pts with HIT. decrease Hgb, Hct.
Canadian trade name Non-Crushable Drug High Alert drug
80 argatroban
A
AVAILABILITY (Rx) 300 sec, give additional bolus 150 mcg/
Infusion (Pre-Mix): 125 mg/125 mL, kg, increase infusion to 30 mcg/kg/min.
250 mg/250 mL. Injection Solution: 250 If ACT is greater than 450 sec, decrease
mg/2.5 mL vial. infusion to 15 mcg/kg/min. Recheck ACT
in 5–10 min. Once ACT of 300–450 sec
ADMINISTRATION/HANDLING achieved, continue dose through dura-
IV
tion of procedure.
Dosage in Renal Impairment
Reconstitution • Dilute each 250-
mg vial with 250 mL 0.9% NaCl, D5W No dose adjustment.
to provide a final concentration of Dosage in Hepatic Impairment
1 mg/mL. Moderate to severe impairment:
Rate of administration • Initial rate ADULTS, ELDERLY: Initially,
0.5 mcg/kg/
of administration is based on body weight min. CHILDREN: Initially, 0.2 mcg/kg/
at 2 mcg/kg/min (e.g., 50-kg pt infuse at min. Adjust dose in increments of 0.05
6 mL/hr). Dosage should not exceed 10 mcg/kg/min or less.
mcg/kg/min.
Storage • Discard if solution ap- SIDE EFFECTS
pears cloudy or an insoluble precipi- Frequent (8%–3%): Dyspnea, hypoten-
tate is noted. • Following reconstitu- sion, fever, diarrhea, nausea, pain, vomit-
tion, stable for 96 hrs at room ing, infection, cough.
temperature or refrigerated. • Avoid
direct sunlight. ADVERSE EFFECTS/
TOXIC REACTIONS
IV INCOMPATIBILITIES
Ventricular tachycardia, atrial fibrillation
Amiodarone (Cardarone).
occur occasionally. Major bleeding, sep-
IV COMPATIBILITIES sis occur rarely.
DiphenhydrAMINE (Benadryl), DOBU-
Tamine (Dobutrex), DOPamine (Intro- NURSING CONSIDERATIONS
pin), furosemide (Lasix), midazolam
BASELINE ASSESSMENT
(Versed), morphine, vasopressin (Pi-
tressin). Refer to IV Compatibility Chart Obtain CBC, PT, aPTT. Determine initial
in front of book. B/P. Minimize need for multiple injection
sites, blood draws, catheters.
INDICATIONS/ROUTES/DOSAGE
INTERVENTION/EVALUATION
Heparin-Induced Thrombocytopenia
(HIT)
Assess for any sign of bleeding: bleed-
IV infusion: ADULTS, ELDERLY: Initially,
ing at surgical site, hematuria, melena,
2 mcg/kg/min administered as a continu- bleeding from gums, petechiae, ecchy-
ous infusion. After initial infusion, dose moses, bleeding from injection sites.
may be adjusted until steady-state aPTT is Handle pt carefully and infrequently to
1.5–3 times initial baseline value, not to prevent bleeding. Assess for decreased
exceed 100 sec. Dosage should not ex- B/P, increased pulse rate, complaint of
ceed 10 mcg/kg/min. abdominal/back pain, severe headache
(may indicate hemorrhage). Monitor
Percutaneous Coronary Intervention ACT, PT, aPTT, platelet count, Hgb, Hct.
IV infusion: ADULTS, ELDERLY: Initially, Question for increase in discharge during
administer bolus of 350 mcg/kg over menses. Assess for hematuria. Observe
3–5 min, then infuse at 25 mcg/kg/min. skin for any occurring ecchymoses, pe-
Check ACT (activated clotting time) 5–10 techiae, hematoma. Use care in removing
min following bolus. If ACT is less than any dressing, tape.
underlined – top prescribed drug
ARIPiprazole 81
A
PATIENT/FAMILY TEACHING with psychotic features, aggression, bipo-
• Use electric razor, soft toothbrush to lar disorder (children), conduct disorder
prevent cuts, gingival trauma. • Report (children), psychosis/agitation related to
any sign of bleeding, including red/dark Alzheimer’s dementia.
urine, black/red stool, coffee-ground
vomitus, blood-tinged mucus from cough. PRECAUTIONS
Contraindications: Hypersensitivity to AR-
IPiprazole. Cautions: Concurrent use of
ARIPiprazole CNS depressants (including alcohol), dis-
orders in which CNS depression is a fea-
ar-i-pip-ra-zole ture, cardiovascular or cerebrovascular
(Abilify, Abilify Maintena, Aristada diseases (may induce hypotension), Par-
Initio) kinson’s disease (potential for exacerba-
tion), history of seizures or conditions that
j BLACK BOX ALERT j Increased may lower seizure threshold (Alzheimer’s
risk of mortality in elderly pts with
dementia-related psychosis, mainly disease), diabetes mellitus. Pts at risk for
due to pneumonia, HF. Increased pneumonia. Elderly with dementia.
risk of suicidal thinking and behav-
ior in children, adolescents, young ACTION
adults 18–24 yrs with major depres-
sive disorder, other psychiatric Provides partial agonist activity at DOPa-
disorders. mine (D2, D3) and serotonin (5-HT1A)
Do not confuse Abilify with receptors and antagonist activity at sero-
Ambien, or ARIPiprazole with tonin (5-HT2A) receptors. Therapeutic
esomeprazole, omeprazole, Effect: Improves symptoms associated
pantoprazole, or RABEprazole with schizophrenia, bipolar disorder, au-
(proton pump inhibitors). tism, depression.
uCLASSIFICATION PHARMACOKINETICS
PHARMACOTHERAPEUTIC: Quin- Well absorbed through GI tract. Pro-
olinone antipsychotic. CLINICAL: Sec- tein binding: 99% (primarily albumin).
ond-generation (atypical) antipsy- Reaches steady levels in 2 wks. Metabo-
chotic agent. lized in liver. Excreted in feces (55%),
urine (25%). Not removed by hemodialy-
sis. Half-life: 75 hrs.
USES
PO: Treatment of schizophrenia. Treat- LIFESPAN CONSIDERATIONS
ment of bipolar disorder. Adjunct treatment Pregnancy/Lactation: Unknown if
in major depressive disorder. Treatment of drug crosses placenta. May be distributed
irritability associated with autism in children in breast milk. Breastfeeding not recom-
6–17 yrs of age. Treatment of Tourette dis- mended. Children: Safety and efficacy
order. IM: (Immediate-Release): Agita- not established. Elderly: May increase
tion associated with schizophrenia/bipolar risk of mortality in pts with dementia-
disorder. (Extended-Release): Abilify related psychosis.
Maintena: Treatment of schizophrenia
in adults. Maintenance monotherapy INTERACTIONS
treatment of bipolar 1 disorder in adults. DRUG: CYP3A4 inducers (e.g., car-
Aristada: Treatment of schizophrenia. BAMazepine, rifampin) may decrease
Aristada Initio: In combination with oral concentration/effect. CYP3A4 inhibitors
aripiprazole for initiation of Aristada when (e.g., erythromycin, ketoconazole,
used for treatment of ­schizophrenia. OFF- ritonavir) may increase concentration/
LABEL: Schizoaffective disorder, depression effect. CNS depressants (e.g., alcohol,
Canadian trade name Non-Crushable Drug High Alert drug
82 ARIPiprazole
A
morphine, oxycodone, zolpidem) INDICATIONS/ROUTES/DOSAGE
may increase CNS depression. Strong Note: May substitute oral solution/tablet
CYP2D6 inhibitors (e.g., fluoxetine, mg per mg up to 25 mg. For 30-mg tab-
paroxetine) may increase concentration/ lets, give 25 mg oral solution.
effect. HERBAL: Herbals with sedative Strong CYP3A4 inducers: ARIPipra-
properties (e.g.,chamomile, kava zole dose should be doubled. Strong
kava, valerian) may increase CNS depres- CYP3A4 inhibitors: ARIPiprazole dose
sion. St. John’s wort may decrease con- should be reduced by 50%.
centration/effect. FOOD: None known. LAB
VALUES: May increase serum glucose. May Schizophrenia
decrease neutrophils, leukocytes. PO: ADULTS, ELDERLY: Initially, 10–15
mg once daily. May increase up to 30
AVAILABILITY (Rx) mg/day. Titrate dose at minimum of 2-wk
Injection, Prefilled Syringe: (Aris- intervals. CHILDREN 13–17 YRS: Initially, 2
tada): 441 mg (1.6 mL), 662 mg (2.4 mg/day for 2 days, then 5 mg/day for 2
mL), 882 mg (3.2 mL), 1064 mg (3.9 days. May further increase to target dose
mL). Injection, Prefilled Syringe: (Abilify of 10 mg/day. May then increase in incre-
Maintena): 300 mg, 400 mg. Injection, ments of 5 mg up to maximum of 30 mg/
Suspension (Extended-Release [Aristada day. IM: ADULTS, ELDERLY: (Abilify Main-
Initio]): 675 mg. Solution, Oral: 1 mg/ tena): Initially, 400 mg monthly (sepa-
mL. Tablets: 2 mg, 5 mg, 10 mg, 15 mg, rate doses by at least 26 days). (Aris-
20 mg, 30 mg. Tablets, Orally Disintegrat- tada): (oral aripiprazole dose: 10 mg/
ing: 10 mg, 15 mg. day) initial IM aripiprazole dose: 441 mg/
mo, (oral aripiprazole dose: 15 mg/day)
ADMINISTRATION/HANDLING 662 mg/mo or 882 mg q6wks or 1,064
IM (Aristada) mg q2mos, (oral aripiprazole dose: 20
• For IM use only (inject slowly into mg or more/day) initial IM aripiprazole
deep muscle mass). Do not administer IV dose 882 mg/mo. Initial IM dose based
or SQ. on oral dose. (In conjunction with first
IM dose, administer oral aripiprazole for
IM (Abilify Maintena) 21 consecutive days.) (Aristada Initio):
Vial • Reconstitute 400-mg vial with 675 mg once (single dose) with 30 mg
1.9 mL Sterile Water for Injection (300- aripiprazole with first IM dose of Aristada.
mg vial with 1.5 mL) to provide a con-
Bipolar Disorder
centration of 100 mg/0.5 mL. Once re-
PO: ADULTS, ELDERLY: Monotherapy:
constituted, administer in gluteal
Initially, 15 mg once daily. May increase
muscle. Do not administer via IV or
to 30 mg/day. Adjunct to lithium or
subcutaneously.
valproic acid: Initially, 10–15 mg.
Prefilled syringe • Reconstitute at
May increase to 30 mg/day based on pt
room temperature by rotating syringe
tolerance. CHILDREN 10–17 YRS: Initially,
plunger to release diluent. Shake until
2 mg/day for 2 days, then 5 mg/day for
suspension is uniform. • Inject full
2 days. May further increase to a target
syringe content immediately following
of 10 mg/day. Give subsequent dose in-
reconstitution.
creases of 5 mg/day. Maximum: 30 mg/
PO day. IM: ADULTS, ELDERLY: (Abilify Main-
• Give without regard to food. tena): Initially, 400 mg monthly (sepa-
rate doses by at least 26 days). Tolerability
Orally Disintegrating Tablet should be established using oral therapy
• Remove tablet, place entire tablet on before initiation of parenteral therapy.
tongue. • Do not break, split tab- Continue oral therapy for 14 days during
let. • May give without liquid. initiation of parenteral therapy.
underlined – top prescribed drug
aspirin 83
A
Major Depressive Disorder (Adjunct to INTERVENTION/EVALUATION
Antidepressants) Periodically monitor weight. Monitor for
PO: ADULTS, ELDERLY: (Abilify): Ini- extrapyramidal symptoms (abnormal
tially, 2–5 mg/day. May increase up to movement), tardive dyskinesia (pro-
maximum of 15 mg/day. Titrate dose in trusion of tongue, puffing of cheeks,
5-mg increments of at least 1-wk intervals. chewing/puckering of the mouth). Peri-
Irritability with Autism
odically monitor B/P, pulse (particularly
PO: CHILDREN 6–17 YRS: Initially, 2 mg/ in pts with preexisting cardiovascular
day for 7 days followed by increase to 5 disease). Monitor serum blood glucose
mg/day. Subsequent increases made in levels during therapy. Assess for thera-
5-mg increments at intervals of at least 1 peutic response (greater interest in sur-
wk. Maximum: 15 mg/day. roundings, improved self-care, increased
ability to concentrate, relaxed facial ex-
Tourette Disorder pression).
PO: CHILDREN 6–17 YRS WEIGHING 50 KG
PATIENT/FAMILY TEACHING
OR MORE: 2 mg/day for 2 days; then 5
mg/day for 5 days with target dose of 10 • Avoid alcohol. • Avoid tasks that re-
mg on day 8. Maximum: 20 mg/day. quire alertness, motor skills until re-
LESS THAN 50 KG: 2 mg/day for 2 days, sponse to drug is established. • Report
then 5 mg/day. Maximum: 10 mg/day. worsening depression, suicidal ideation,
unusual changes in behavior, extrapyra-
Dosage in Renal/Hepatic Impairment midal effects.
No dose adjustment.
SIDE EFFECTS aspirin
Frequent (11%–5%): Weight gain, head-
ache, insomnia, vomiting. Occasional (4%– as-pir-in
3%): Light-headedness, nausea, akathisia, (Asaphen E.C. , Ascriptin, Bayer,
drowsiness. Rare (2% or less): Blurred Bufferin, Durlaza, Ecotrin, Entro-
vision, constipation, asthenia (loss of phen , Novasen )
strength, energy), anxiety, fever, rash, Do not confuse aspirin or
cough, rhinitis, orthostatic hypotension. Ascriptin with Afrin, Aricept, or
Ecotrin with Epogen.
ADVERSE EFFECTS/TOXIC
REACTIONS FIXED-COMBINATION(S)
Extrapyramidal symptoms, neuroleptic Aggrenox: aspirin/dipyridamole (an
malignant syndrome, tardive dyskinesia, antiplatelet agent): 25 mg/200 mg.
hyperglycemia, ketoacidosis, hyperosmo- Fiorinal: aspirin/butalbital/caffeine
lar coma, CVA, TIA occur rarely. Prolonged (a barbiturate): 325 mg/50 mg/40 mg.
QT interval occurs rarely. May cause leu- Lortab/ASA: aspirin/HYDROcodone
kopenia, neutropenia, agranulocytosis. (an analgesic): 325 mg/5 mg. Perco-
dan: aspirin/oxyCODONE (an anal-
NURSING CONSIDERATIONS gesic): 325 mg/2.25 mg, 325 mg/4.5
BASELINE ASSESSMENT mg. Pravigard: aspirin/pravastatin
Assess behavior, appearance, emotional (a cholesterol-lowering agent): 81
status, response to environment, speech pat- mg/20 mg, 81 mg/40 mg, 81 mg/80
tern, thought content. Correct dehydration, mg, 325 mg/20 mg, 325 mg/40 mg,
hypovolemia. Assess for suicidal tendencies. 325 mg/80 mg. Yosprala: aspirin/
Question history (or family history) of dia- omeprazole (a proton pump inhibitor
betes. Obtain serum blood glucose level. [PPI]) 325 mg/40 mg, 81 mg/40 mg.

Canadian trade name Non-Crushable Drug High Alert drug


84 aspirin
A
uCLASSIFICATION PHARMACOKINETICS
PHARMACOTHERAPEUTIC: Non- Route Onset Peak Duration
steroidal anti-inflammatory drug PO 1 hr 2–4 hrs 4–6 hrs
(NSAID). CLINICAL: Anti-inflammato-
ry, antipyretic, analgesic, anti-platelet. Rapidly and completely absorbed from GI
tract; enteric-coated absorption delayed;
rectal absorption delayed and incom-
USES plete. Protein binding: High. Widely dis-
Treatment of mild to moderate pain, tributed. Rapidly hydrolyzed to salicylate.
fever. Reduces inflammation related to Half-life: 15–20 min (aspirin); 2–3
rheumatoid arthritis (RA), juvenile ar- hrs (salicylate at low dose); more than
thritis, osteoarthritis, rheumatic fever. 20 hrs (salicylate at high dose).
Used as platelet aggregation inhibitor
in the prevention of transient ischemic LIFESPAN CONSIDERATIONS
attacks (TIAs), cerebral thromboembo- Pregnancy/Lactation: Readily crosses
lism, MI or reinfarction. Durlaza: Re- placenta; distributed in breast milk. May
duce risk of MI in pts with CAD or stroke prolong gestation and labor, decrease
in pts who have had TIA or ischemic fetal birth weight, increase incidence of
stroke. OFF-LABEL: Prevention of pre- stillbirths, neonatal mortality, hemor-
eclampsia; alternative therapy for pre- rhage. Avoid use during last trimester
venting thromboembolism associated (may adversely affect fetal cardiovascular
with atrial fibrillation when warfarin can- system: premature closure of ductus ar-
not be used; pericarditis associated with teriosus). Children: Caution in pts with
MI; prosthetic valve thromboprophylaxis. acute febrile illness (Reye’s syndrome).
Adjunctive treatment of Kawasaki’s dis- Elderly: May be more susceptible to
ease. Complications associated with au- toxicity; lower dosages recommended.
toimmune disorders, colorectal cancer.
INTERACTIONS
PRECAUTIONS DRUG: Alcohol, NSAIDs (e.g., ibu-
Contraindications: Hypersensitivity to profen, ketorolac, naproxen) may
NSAIDs. Pts with asthma r­hinitis, n­asal increase risk of GI effects (e.g., ulcer-
polyps; inherited or acquired bleed- ation). Antacids, urinary alkalinizers
ing disorders; use in children (younger increase excretion. Anticoagulants,
than 16 yrs) for viral infections with or (e.g. enoxaparin, warfarin), hepa-
without fever. Cautions: Platelet/bleeding rin, thrombolytics, ticagrelor increase
disorders, severe renal/hepatic impair- risk of bleeding. Apixaban, dabigatran,
ment, dehydration, erosive gastritis, pep- edoxaban, rivaroxaban may increase
tic ulcer disease, sensitivity to tartrazine anticoagulant effect. HERBAL: Herbals
dyes, elderly (chronic use of doses 325 with anticoagulant/antiplatelet prop-
mg or greater). Avoid use in pregnancy, erties (e.g., garlic, ginger, ginkgo
especially third trimester. biloba) may increase risk of bleeding.
FOOD: None known. LAB VALUES: May
ACTION alter serum ALT, AST, alkaline phospha-
Irreversibly inhibits cyclo-oxygenase en- tase, uric acid; prolongs prothrombin time
zyme, resulting in a decreased formation (PT) platelet function assay. May decrease
of prostaglandin precursors. Irreversibly serum cholesterol, potassium, T3, T4.
inhibits formation of thromboxane, re-
sulting in inhibiting platelet aggregation. AVAILABILITY (OTC)
Therapeutic Effect: Reduces inflamma- Caplets: 325 mg, 500 mg. Supposito-
tory response, intensity of pain; decreases ries: 300 mg, 600 mg. Tablets: 325 mg.
fever; inhibits platelet aggregation. Tablets (Chewable): 81 mg.

underlined – top prescribed drug


aspirin 85
A
Capsule, Extended-Release: (Durlaza) mild nausea); allergic reaction (includ-
162.5 mg. Tablets (Enteric-Coated): 81 mg, ing bronchospasm, pruritus, urticaria).
325 mg, 500 mg, 650 mg.
ADVERSE EFFECTS/
ADMINISTRATION/HANDLING TOXIC REACTIONS
PO High doses of aspirin may produce GI
• Do not break, crush, dissolve, or di- bleeding and/or gastric mucosal lesions.
vide enteric-coated tablets or extended- Dehydrated, febrile children may expe-
release capsule. • May give with water, rience aspirin toxicity quickly. Reye’s
milk, meals if GI distress occurs. syndrome, characterized by persistent
vomiting, signs of brain dysfunction,
Rectal may occur in children taking aspirin
• Refrigerate suppositories; do not with recent viral infection (chickenpox,
freeze. • If suppository is too soft, chill common cold, or flu). Low-grade as-
for 30 min in refrigerator or run cold pirin toxicity characterized by tinnitus,
water over foil wrapper. • Moisten generalized pruritus (may be severe),
­suppository with cold water before in- headache, dizziness, flushing, tachy-
serting well into rectum. cardia, hyperventilation, diaphoresis,
thirst. Marked toxicity characterized
INDICATIONS/ROUTES/DOSAGE by hyperthermia, restlessness, seizures,
Analgesia, Fever abnormal breathing patterns, respira-
PO: ADULTS, ELDERLY, CHILDREN 12 YRS tory failure, coma.
AND OLDER AND WEIGHING 50 KG OR
MORE: 325–650 mg q4–6h or 975 mg NURSING CONSIDERATIONS
q6h prn or 500–1,000 mg q4–6h prn.
BASELINE ASSESSMENT
Maximum: 4 g/day. RECTAL: 300–
600 mg q4h prn. INFANTS, CHILDREN Do not give to children or teenagers
WEIGHING LESS THAN 50 KG: 10–15 mg/ who have or have recently had viral
kg/dose q4–6h. Maximum: 4 g/day or infections (increases risk of Reye’s
90 mg/kg/day. syndrome). Do not use if vinegar-like
odor is noted (indicates chemical
Revascularization breakdown). Assess history of GI bleed,
PO: ADULTS, ELDERLY: 80–325 mg/day. peptic ulcer disease, OTC use of prod-
ucts that may contain aspirin. Assess
Kawasaki’s Disease type, location, duration of pain, inflam-
PO: CHILDREN: 80–100 mg/kg/day in mation. Inspect appearance of affected
divided doses q6h up to 14 days (until joints for immobility, deformities, skin
fever resolves for at least 48 hrs). After condition. Therapeutic serum level
fever resolves, 1–5 mg/kg once daily for for antiarthritic effect: 20–30 mg/
at least 6–8 wks. dL (toxicity occurs if level is greater
than 30 mg/dL).
MI, Stroke (Risk Reduction)
INTERVENTION/EVALUATION
PO: ADULTS, ELDERLY: (Durlaza): 162.5 mg
once daily. Monitor urinary pH (sudden acidifica-
tion, pH from 6.5 to 5.5, may result in
Dosage in Renal/Hepatic Impairment toxicity). Assess skin for evidence of
Avoid use in severe impairment. ecchymosis. If given as antipyretic, as-
sess temperature directly before and 1
SIDE EFFECTS hr after giving medication. Evaluate for
therapeutic response: relief of pain, stiff-
Occasional: GI distress (including ab-
ness, swelling; increased joint mobility;
dominal distention, cramping, heartburn,
Canadian trade name Non-Crushable Drug High Alert drug
86 atazanavir
A
reduced joint tenderness; improved grip renal ­ impairment (not recommended
strength. in end-stage renal disease or pts on he-
modialysis), hemophilia A or B, hepatitis
PATIENT/FAMILY TEACHING
B or C virus infection. Do not use in pts
• Do not, chew, crush, dissolve, or di- younger than 3 mos (potential for kernic-
vide enteric-coated tablets. • Avoid al- terus). Pts with increased transaminase
cohol, OTC pain/cold products that may levels prior to use or underlying hepatic
contain aspirin. • Report ringing of the ­disease.
ears or persistent abdominal GI pain,
bleeding. • Therapeutic anti-inflamma- ACTION
tory effect noted in 1–3 wks. • Behav- Binds to HIV-1 protease, inhibiting cleav-
ioral changes, persistent vomiting may be age of viral precursors into functional
early signs of Reye’s syndrome; contact proteins required for infectious HIV.
physician. Therapeutic Effect: Prevents forma-
tion of mature HIV viral cells.
PHARMACOKINETICS
atazanavir Rapidly absorbed after PO administration.
Protein binding: 86%. Extensively me-
a-ta-zan-a-veer tabolized in liver. Excreted in feces (79%),
(Reyataz) urine (13%). Half-life: 5–8 hrs.
Do not confuse Reyataz with
Retavase. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if
FIXED-COMBINATION(S) drug crosses placenta or is distributed
Evotaz: atazanavir/cobicistat (anti- in breast milk. Lactic acidosis syndrome,
retroviral booster): 300 mg/150 mg. hyperbilirubinemia, kernicterus have
been reported. Children: Safety and ef-
uCLASSIFICATION
ficacy not established in pts younger than
PHARMACOTHERAPEUTIC: Antiret- 3 mos. Elderly: Age-related hepatic
roviral. CLINICAL: Protease inhibitor. impairment may require dose reduction.
INTERACTIONS
USES
DRUG: May increase concentration, tox-
Treatment of HIV-1 infection in combina- icity of amiodarone, atorvastatin, be-
tion with at least two other antiretroviral pridil, clarithromycin, cycloSPORINE,
agents in pts 3 mos and older, weighing diltiaZEM, lovastatin, rosuvastatin,
5 kg or more. sildenafil, simvastatin, sirolimus,
tacrolimus, tadalafil, tricyclic antide-
PRECAUTIONS
pressants, vardenafil, verapamil, war-
Contraindications: Hypersensitivity to farin. H2-receptor antagonists, pro-
atazanavir. Concurrent use with alfuzosin, ton pump inhibitors, rifAMPin may
ergot derivatives, indinavir, irinotecan, decrease concentration/effects. Ritonavir,
lovastatin, lurasidone (when atazanavir voriconazole may increase concentra-
given with ritonavir), midazolam (oral), tion. HERBAL: St. John’s wort may de-
nevirapine, pimozide, rifAMPin, sildenafil crease concentration/effect. FOOD: High-
(for pulmonary arterial hypertension), fat meals may decrease absorption. LAB
St. John’s wort, simvastatin, triazolam. VALUES: May increase serum bilirubin,
Cautions: Preexisting conduction sys- ALT, AST, amylase, lipase. May decrease
tem defects (first-, second-, or third- Hgb, neutrophil count, platelets. May alter
degree AV block), diabetes, elderly, LDL, triglycerides.

underlined – top prescribed drug


atazanavir 87
A
AVAILABILITY (Rx) HIV-1 Infection (Concurrent Therapy with
Tenofovir)
Capsules: 150 mg, 200 mg, 300 mg.
PO: ADULTS, ELDERLY: 300 mg atazanavir,
Packet, Oral: 50 mg.
100 mg ritonavir, and 300 mg tenofovir given
ADMINISTRATION/HANDLING as a single daily dose with food. FOR TREAT-
MENT-EXPERIENCED PREGNANT WOMEN DUR-
PO
ING SECOND OR THIRD TRIMESTER: 400 mg
• Give with food. • Swallow whole; do
not break or open capsules. • Administer and ritonavir 100 mg once daily.
at least 2 hrs before or 10 hrs after H2 an- HIV-1 Infection in Pts with Mild to
tagonist, 12 hrs after proton pump inhibitor. Moderate Hepatic Impairment
INDICATIONS/ROUTES/DOSAGE b ALERT c Avoid use in pts with severe
Note: Dosage adjustment may be necessary hepatic impairment.
PO: ADULTS, ELDERLY: 300 mg once
with colchicine, bosentan, H2 ­antagonists,
proton pump inhibitors, PDE5 inhibitors. daily with food.

HIV-1 Infection Dosage in Renal Impairment


PO: ADULTS, ELDERLY (ANTIRETROVIRAL- HD: (NAÏVE): 300 mg with ritonavir. (EXPE-
NAÏVE): 300 mg and ritonavir 100 mg, RIENCED): Not recommended.
or cobicistat 150 mg, once daily, or 400
mg (2 capsules) once daily with food in SIDE EFFECTS
pts unable to tolerate ritonavir. ADULTS, EL- Frequent (16%–14%): Nausea, headache.
DERLY (ANTIRETROVIRAL-EXPERIENCED): 300 Occasional (9%–4%): Rash, vomiting,
mg and ritonavir 100 mg, or cobicistat 150 depression, diarrhea, abdominal pain,
mg, once daily. PREGNANT PTS (NAÏVE OR fever. Rare (3% or less): Dizziness, in-
EXPERIENCED): 300 mg and ritonavir 100 somnia, cough, fatigue, back pain.
mg once daily. CHILDREN 6–17 YRS (NAÏVE
OR EXPERIENCED) WEIGHING 35 KG OR MORE:
ADVERSE EFFECTS/
Capsules: 300 mg once daily (with ritona-
TOXIC REACTIONS
vir 100 mg). WEIGHING 15–34 KG: 200 mg Severe hypersensitivity reaction (angio-
once daily (with ritonavir 100 mg). edema, chest pain), jaundice may occur.
Powder (naïve and experienced):
CHILDREN WEIGHING 25 KG OR MORE: 300 NURSING CONSIDERATIONS
mg (6 packets) plus ritonavir 100 mg
BASELINE ASSESSMENT
once daily. WEIGHING 15–24 KG: 250 mg (5
packets) plus ritonavir 80 mg once daily. Obtain baseline CBC, BMP, LFT, viral load
WEIGHING 5–14 KG: 200 mg (4 packets) before beginning therapy and at periodic
plus ritonavir 80 mg once daily. intervals during therapy. Offer emotional
support.
HIV-1 Infection (Concurrent Therapy with
INTERVENTION/EVALUATION
Efavirenz)
PO: ADULTS, ELDERLY: 400 mg atazana- Monitor lab results. Assess for nausea,
vir, 100 mg ritonavir (as a single dose vomiting; assess eating pattern. Monitor
given with food), and 600 mg efavirenz as daily pattern of bowel activity, stool con-
a single daily dose on an empty stomach sistency. Assess skin for rash. Question
(preferably at bedtime). for evidence of headache. Assess mood
for evidence of depression.
HIV-1 Infection (Concurrent Therapy with PATIENT/FAMILY TEACHING
Didanosine)
• Take with food. • Small, frequent
PO: ADULTS, ELDERLY: Give atazanavir with
meals may offset nausea, vomit-
food 2 hrs before or 1 hr after didanosine.
ing. • Swallow whole; do not break or
Canadian trade name Non-Crushable Drug High Alert drug
88 atenolol
A
open capsules. • Pt must continue history of anaphylaxis to allergens, con-
practices to prevent HIV transmis- current use with digoxin, verapamil, or
sion. • Atazanavir is not a cure for HIV diltiaZEM.
infection, nor does it reduce risk of
transmission to others. • Report dizzi- ACTION
ness, light-headedness, yellowing of skin Blocks beta1-adrenergic receptors in car-
or whites of eyes, flank pain or when diac tissue. Therapeutic Effect: Slows
urinating, blood in urine, skin rash. sinus node heart rate, decreasing cardiac
output, B/P. Decreases myocardial oxy-
gen demand.

atenolol PHARMACOKINETICS
Route Onset Peak Duration
a-ten-oh-lol PO 1 hr 2–4 hrs 24 hrs
(Tenormin)
j BLACK BOX ALERT jDo not Incompletely absorbed from GI tract. Pro-
abruptly discontinue; taper gradu- tein binding: 6%–16%. Minimal liver me-
ally to avoid acute tachycardia, tabolism. Primarily excreted unchanged
hypertension, ischemia. in urine. Removed by hemodialysis.
Do not confuse atenolol with Half-life: 6–9 hrs (increased in renal
albuterol, timolol, or Tylenol, impairment).
or Tenormin with Imuran,
Norpramin, or thiamine. LIFESPAN CONSIDERATIONS
uCLASSIFICATION
Pregnancy/Lactation: Readily crosses
placenta; distributed in breast milk.
PHARMACOTHERAPEUTIC: Beta 1 - Avoid use during first trimester. May pro-
adrenergic blocker. CLINICAL: An- duce bradycardia, apnea, hypoglycemia,
tihypertensive, antianginal, antiar- hypothermia during delivery; low birth-
rhythmic. weight infants. Children: No age-related
precautions noted. Elderly: Age-related
USES peripheral vascular disease, renal im-
pairment require ­caution.
Treatment of hypertension, alone or in
combination with other agents; manage- INTERACTIONS
ment of angina pectoris; management of DRUG: Alpha2 agonists (e.g., cloni-
pts with definite/suspected MI to reduce dine) may increase AV-blocking effect.
CV mortality. OFF-LABEL: Arrhythmia Strong CYP3A4 inducers (e.g., car-
(esp. supraventricular and ventricular bamazepine, rifampin) may decrease
tachycardia), thyrotoxicosis. concentration/effect. Dronedarone,
PRECAUTIONS fingolimod, rivastigmine may in-
crease bradycardic effect. May increase
Contraindications: Hypersensitivity to vasoconstriction of ergot derivatives
atenolol. Cardiogenic shock, uncom- (e.g., dihydroergotamine, ergota-
pensated HF, second- or third-degree mine). HERBAL: Herbals with hyper-
heart block (except with functioning tensive properties (e.g., licorice,
pacemaker), sinus bradycardia, sinus yohimbe) or hypotensive proper-
node dysfunction. Cautions: Elderly, ties (e.g., garlic, ginger, ginkgo bi-
renal impairment, peripheral vascular loba) may alter effects. St. John’s wort
disease, diabetes, thyroid disease, bron- may decrease concentration/effect.
chospastic disease, compensated HF, FOOD: None known. LAB VALUES: May
myasthenia gravis, psychiatric disease,

underlined – top prescribed drug


atenolol 89
A
increase serum ANA titer, serum BUN, somnia, flatulence, urinary frequency, im-
creatinine, potassium, uric acid, lipo- potence or decreased libido, depression.
protein, triglycerides. Rare: Rash, arthralgia, myalgia, confusion
(esp. in the elderly), altered taste.
AVAILABILITY (Rx)
Tablets: 25 mg, 50 mg, 100 mg. ADVERSE EFFECTS/
TOXIC REACTIONS
ADMINISTRATION/HANDLING Overdose may produce profound brady-
PO cardia, hypotension. Abrupt withdrawal
• Give without regard to food. • Tab- may result in diaphoresis, palpitations,
lets may be crushed. headache, tremors. May precipitate HF,
MI in pts with cardiac disease; thyroid
INDICATIONS/ROUTES/DOSAGE storm in pts with thyrotoxicosis; periph-
Hypertension eral ischemia in pts with existing periph-
PO: ADULTS: Initially, 25–50 mg once eral vascular disease. Hypoglycemia may
daily. After 1–2 wks, may increase dose occur in previously controlled diabetes.
up to 100 mg once daily. ELDERLY: Usual Thrombocytopenia (unusual bruising,
initial dose, 25 mg/day. CHILDREN: Ini- bleeding) occurs rarely. Antidote: Glu-
tially, 0.5–1 mg/kg/dose given once cagon (see Appendix J for dosage).
daily. Range: 0.5–1.5 mg/kg/day. Maxi-
mum: 2 mg/kg/day up to 100 mg/day. NURSING CONSIDERATIONS
Angina Pectoris BASELINE ASSESSMENT
PO: ADULTS: Initially, 50 mg once daily. Assess B/P, apical pulse immediately before
May increase dose up to 200 mg once daily. drug is administered (if pulse is 60/min or
ELDERLY: Usual initial dose, 25 mg/day. less, or systolic B/P is less than 90 mm Hg,
withhold medication, contact physician).
Post-MI Antianginal: Record onset, quality (sharp,
PO: ADULTS: 100 mg once daily or 50 dull, squeezing), radiation, location, inten-
mg twice daily. Begin within first 24 hrs sity, duration of anginal pain, precipitating
post-MI, then continue indefinitely. factors (exertion, emotional stress). Assess
Dosage in Renal Impairment baseline renal/hepatic function tests.
Dosage interval is modified based on cre- INTERVENTION/EVALUATION
atinine clearance. Monitor B/P for hypotension, pulse for
Creatinine Maximum bradycardia, respiration for difficulty in
Clearance Dosage breathing, ECG. Monitor daily pattern of
15–35 mL/min 50 mg/day bowel activity, stool consistency. Assess
Less than 15 mL/min 25 mg/day for evidence of HF: dyspnea (particularly
Hemodialysis (HD) Give dose post-HD on exertion or lying down), nocturnal
or give 25–50 mg cough, peripheral edema, distended neck
supplemental dose veins. Monitor I&O (increased weight,
Dosage in Hepatic Impairment decreased urinary output may indicate
No dose adjustment. HF). Assess extremities for pulse quality,
changes in temperature (may indicate
SIDE EFFECTS worsening peripheral vascular disease).
Atenolol is generally well tolerated, with mild Assist with ambulation if dizziness occurs.
and transient side effects. Frequent: Hypo- PATIENT/FAMILY TEACHING
tension manifested as cold extremities, con-
stipation or diarrhea, diaphoresis, dizziness, • Do not abruptly discontinue medica-
fatigue, headache, nausea. Occasional: In- tion. • Compliance with therapy essen-
tial to control hypertension, angina. • To

Canadian trade name Non-Crushable Drug High Alert drug


90 atezolizumab
A
reduce hypotensive effect, go from lying to of extensive-stage small-cell lung cancer
standing slowly. • Avoid tasks that re- (in combination with carboplatin and
quire alertness, motor skills until re- etoposide).
sponse to drug is established. • Advise
diabetic pts to monitor blood glucose PRECAUTIONS
carefully (may mask signs of hypoglyce- Contraindications: Hypersensitivity to
mia). • Report dizziness, depression, atezolizumab. Cautions: Active infection;
confusion, rash, unusual bruising/bleed- baseline anemia, lymphopenia; diabetes;
ing. • Outpatients should monitor B/P, pts at risk for dehydration, electrolyte
pulse before taking medication, following imbalance; hepatic impairment, periph-
correct technique. • Restrict salt, alco- eral or generalized edema, neuropathy,
hol intake. • Therapeutic antihyperten- optic disorders, interstitial lung disease;
sive effect noted in 1–2 wks. history of venous thromboembolism, in-
testinal obstruction, pancreatitis.
ACTION
atezolizumab Binds to PD-L1 to selectively prevent
the interaction between PD-L1 and B7.1
a-te-zoe-liz-ue-mab ­receptors. PD-L1 is an immune check-
(Tecentriq) point protein expressed on tumor cells.
Do not confuse atezolizumab Therapeutic Effect: Restores anti-
with daclizumab, certolizumab, tumor T-cell function.
eculizumab, omalizumab, or
tocilizumab. PHARMACOKINETICS
Metabolism not specified. Steady state
uCLASSIFICATION
reached in 6–9 wks. Elimination not
PHARMACOTHERAPEUTIC: Pro- specified. Half-life: 27 days.
grammed death-ligand 1 (PD-L1)
blocking antibody. Monoclonal anti- LIFESPAN CONSIDERATIONS
body. CLINICAL: Antineoplastic. Pregnancy/Lactation: Avoid preg-
nancy; may cause fetal harm. Unknown
if distributed in breast milk; however,
USES human immunoglobulin G is present in
Treatment of pts with locally advanced or breast milk. Breastfeeding not recom-
metastatic urothelial carcinoma who have mended during treatment and for at least
disease progression during or following 5 mos after discontinuation. Females of
platinum-containing chemotherapy or reproductive potential should use ef-
have disease progression within 12 mos fective contraception during treatment
of neoadjuvant or adjuvant treatment and up to 5 mos after discontinuation.
with platinum-containing chemotherapy. May impair fertility in females. Chil-
Treatment of metastatic NSCLC in pts with dren: Safety and efficacy not estab-
disease progression during or following lished. Elderly: No age-related precau-
platinum-containing chemotherapy. Pts tions noted.
should have disease progression on ap-
proved therapy for EGFR or ALK genomic INTERACTIONS
tumor mutation before receiving atezoli- DRUG: None known. HERBAL: None sig-
zumab. Treatment of unresectable locally nificant. FOOD: None known. LAB VAL-
advanced or metastatic triple-negative UES: May increase serum alkaline phos-
breast cancer (in combination with pacli- phatase, ALT, AST, creatinine, glucose.
taxel [protein bound]) in pts whose tu- May decrease serum albumin, sodium;
mors express PD-L1. First-line treatment lymphocytes, Hgb, Hct, RBCs.
underlined – top prescribed drug
atezolizumab 91
A
AVAILABILITY (Rx) Breast Cancer (Triple-Negative), Locally
Advanced or Metastatic
Injection Solution: 1,200 mg/20 mL (60
IV: ADULTS, ELDERLY: 840 mg on days 1
mg/mL).
and 15 q4wks (in combination with pa-
ADMINISTRATION/HANDLING clitaxel [protein bound]) until disease
progression or unacceptable toxicity.
IV
Small-Cell Lung Cancer (Extensive-Stage),
Reconstitution • Visually inspect so- First-Line Treatment
lution for particulate matter or discolor- IV: ADULTS, ELDERLY: Induction: 1,200
ation. Solution should appear clear to mg on day 1 q3wks (in combination
slightly yellow. Discard if solution is with carboplatin and etoposide) for 4
cloudy or discolored or if visible parti- cycles, followed by single-agent mainte-
cles are present. • Do not shake nance therapy of 840 mg once q2wks; or
vial. • Withdraw 20 mL of solution from 1,200 mg once q3wks; or 1,680 mg once
vial and dilute into a 250-mL polyvinyl q4wks. Continue until disease progres-
chloride, polyethylene, or polyolefin infu- sion or unacceptable toxicity.
sion bag containing 0.9% NaCl. Dilute
with 0.9% NaCl only. • Mix by gentle Dose Modification
inversion. • Do not shake. • Discard Based on Common Terminology Criteria
partially used or empty vials. for Adverse Events (CTCAE). Withhold
Rate of administration • Infuse over treatment for any of the following
60 min using sterile, nonpyrogenic, low toxic reactions: Grade 2 or 3 diarrhea
protein-binding, 0.2- to 0.22-micron in-line or colitis; Grade 2 pneumonitis; serum
filter. • If first infusion is tolerated, all AST or ALT elevation 3–5 times upper
subsequent infusions may be delivered over limit of normal (ULN) or serum bilirubin
30 mins. • Do not administer as IV bolus. elevation 1.5–3 times ULN; symptomatic
Storage • Refrigerate diluted solution hypophysitis, adrenal insufficiency, hypo-
up to 24 hrs or store at room tempera- thyroidism, hyperthyroidism; Grade 3 or
ture for no more than 6 hrs (includes 4 hyperglycemia; Grade 3 rash; Grade 2
time of preparation and infusion). • Do ocular inflammatory toxicity, Grade 2 or
not freeze. • Do not shake. 3 pancreatitis, Grade 3 or 4 infection,
Grade 2 infusion-related reactions. Re-
IV INCOMPATIBILITIES starting treatment after interruption
Do not administer with other medica- of therapy: Resume treatment when
tions. Infuse via dedicated line. adverse effects return to Grade 0 or 1.
Permanently discontinue for any of
INDICATIONS/ROUTES/DOSAGE the following toxic reactions: Grade
NSCLC 3 or 4 diarrhea or colitis; Grade 3 or 4
IV: ADULTS, ELDERLY: 1,200 mg on day pneumonitis; serum AST or ALT eleva-
1 q3wks (followed by bevacizumab, tion greater than 5 times ULN or serum
paclitaxel, carboplatin) for 4–6 cycles, bilirubin elevation 3 times ULN; Grade 4
then 1,200 mg on day 1 (followed by hypophysitis; Grade 4 rash; Grade 3 or 4
bevacizumab) q3wks. Continue until ocular inflammatory toxicity; Grade 4 or
disease progression or unacceptable any grade recurrent pancreatitis; Grade 3
toxicity. or 4 infusion-related reactions; any oc-
currence of encephalitis, Guillain-Barré,
Urothelial Carcinoma meningitis, meningoencephalitis, myas-
IV: ADULTS, ELDERLY: 1,200 mg q3wks thenic syndrome/myasthenia gravis.
until disease progression or unaccept-
able toxicity. No dose reductions are rec- Dosage in Renal Impairment
ommended. No dose adjustment.
Canadian trade name Non-Crushable Drug High Alert drug
92 atezolizumab
A
Dosage in Hepatic Impairment pulmonary/thyroid disease, autoimmune
Mild impairment: No dose adjustment. disorders, diabetes, hepatic impairment,
Moderate to severe impairment: Not venous thromboembolism. Conduct full
specified; use caution. dermatologic/neurologic/ophthalmo-
logic exam. Verify use of effective con-
SIDE EFFECTS traception in females of reproductive po-
Frequent (52%–18%): Fatigue, decreased tential. Screen for active infection. Assess
appetite, nausea, pyrexia, constipation, hydration status.
diarrhea, peripheral edema. Occasional
INTERVENTION/EVALUATION
(17%–13%): Abdominal pain, vomiting,
dyspnea, back/neck pain, rash, arthral- Monitor CBC, BMP, LFT, thyroid panel,
gia, cough, pruritus. vital signs. Diligently monitor for im-
mune-mediated adverse events as listed
ADVERSE EFFECTS/TOXIC in Adverse Effects/Toxic Reactions. Notify
REACTIONS physician if any CTCAE toxicities occur,
May cause severe immune-mediated and initiate proper treatment. Obtain
events including adrenal insufficiency chest X-ray if interstitial lung disease,
(0.4% of pts), interstitial lung disease pneumonitis suspected. Due to high risk
or pneumonitis (3% of pts), colitis or for dehydration/diarrhea, strictly moni-
diarrhea (20% of pts), hepatitis (2%– tor I&O. Encourage PO intake. If cortico-
3% of pts), hypophysitis (0.2% of pts), steroid therapy is initiated for immune-
hyperthyroidism (1% of pts), hypothy- mediated events, monitor capillary blood
roidism (4% of pts), rash (up to 37% of glucose and screen for corticosteroid
pts), new-onset diabetes with ketoacido- side effects. Report any changes in neu-
sis (0.2% of pts), pancreatitis (0.1% of rologic status, including nuchal rigidity
pts); meningoencephalitis, myasthenic with fever, positive Kernig’s sign, positive
syndrome/myasthenia gravis, Guillain- Brudzinski’s sign, altered mental status,
Barré, ocular inflammatory toxicity (less seizures. Diligently monitor for infection.
than 1% of pts). Severe, sometimes fa- PATIENT/FAMILY TEACHING
tal infections, including sepsis, herpes
encephalitis, mycobacterial infection, • Blood levels will be routinely moni-
occurred in 38% of pts. Urinary tract tored. • Avoid pregnancy; treatment
infections were the most common cause may cause birth defects. Do not breast-
of Grade 3 or higher infection, occur- feed. Females of childbearing potential
ring in 7% of pts. Severe infusion-related should use effective contraception during
reactions reported in less than 1% of treatment and for at least 5 mos after fi-
pts. Other adverse events, including nal dose. • Treatment may cause seri-
acute kidney injury, dehydration, dys- ous or life-threatening inflammatory re-
pnea, ­encephalitis, hematuria, intestinal actions. Report signs and symptoms of
obstruction, meningitis, neuropathy, treatment-related inflammatory events in
pneumonia, urinary obstruction, venous the following body systems: colon (se-
thromboembolism, were reported. Im- vere abdominal pain or diarrhea); eye
munogenicity (auto-atezolizumab anti- (blurry vision, double vision, unequal
bodies) occurred in 42% of pts. pupil size, sensitivity to light, eyelid
drooping); lung (chest pain, cough,
NURSING CONSIDERATIONS shortness of breath); liver (bruising eas-
ily, amber-colored urine, clay-colored/
BASELINE ASSESSMENT tarry stools, yellowing of skin or eyes);
Obtain baseline CBC, BMP, LFT, thyroid pituitary (persistent or unusual head-
panel, urine pregnancy, urinalysis; vi- ache, dizziness, extreme weakness, faint-
tal signs. Screen for history of pituitary/ ing, vision changes); thyroid (trouble

underlined – top prescribed drug


atoMOXetine 93
A
sleeping, high blood pressure, fast heart ACTION
rate [overactive thyroid]), (fatigue, goi- Selectively inhibits reuptake of norepi-
ter, weight gain [underactive thyroid]), nephrine. Therapeutic Effect: Im-
neurologic (confusion, headache, sei- proves symptoms of ADHD.
zures, neck rigidity with fever, severe
nerve pain or loss of motor func- PHARMACOKINETICS
tion). • Immediately report allergic re- Rapidly absorbed after PO administra-
actions, bleeding of any kind, signs of tion. Protein binding: 98% (primarily
infection. • Treatment may cause se- to albumin). Excreted in urine (80%),
vere diarrhea. Drink plenty of fluids. feces (17%). Not removed by hemodi-
alysis. Half-life: 4–5 hrs (increased
in moderate to severe hepatic insuffi-
atoMOXetine ciency).
LIFESPAN CONSIDERATIONS
at-oh-mox-e-teen
(Apo-Atomoxetine , Strattera) Pregnancy/Lactation: Unknown if dis-
tributed in breast milk. Children: Safety
j BLACK BOX ALERT j Increased and efficacy not established in pts
risk of suicidal thinking and be-
havior in children and adolescents younger than 6 yrs. May produce suicidal
with attention-deficit hyperactivity thoughts in children and adolescents.
disorder (ADHD). ­ lderly: Age-related hepatic/renal im-
E
Do not confuse atomoxetine pairment, cardiovascular or cerebrovas-
with atorvastatin. cular disease may increase risk of adverse
effects.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Norepi- INTERACTIONS
nephrine reuptake inhibitor. CLINICAL: DRUG: MAOIs may increase concentra-
Psychotherapeutic agent. tion/effect. Strong CYP2D6 inhibi-
tors (e.g., FLUoxetine, paroxetine)
USES may increase concentration/effect.
HERBAL: None significant. FOOD: None
Treatment of ADHD. known. LAB VALUES: May increase he-
patic enzymes, serum bilirubin.
PRECAUTIONS
Contraindications: Hypersensitivity to AVAILABILITY (Rx)
atomoxetine. Narrow-angle glaucoma, Capsules: 10 mg, 18 mg, 25 mg, 40 mg,
use with or within 14 days of MAOIs. 60 mg, 80 mg, 100 mg.
Pheochromocytoma or history of pheo-
chromocytoma. Severe cardiovascular ADMINISTRATION/HANDLING
or vascular disease. Cautions: Hyperten- PO
sion, tachycardia, cardiovascular disease • Give without regard to food. • Swal-
(e.g., structural abnormalities, cardio- low capsules whole, do not break or open
myopathy), urinary retention, moderate (powder in capsule is ocular irritant).
or severe hepatic impairment, suicidal Give as single daily dose in the morning or
ideation, emergent psychotic or manic 2 evenly divided doses in morning and late
symptoms, comorbid bipolar disorder, afternoon/early ­evening.
renal impairment, poor metabolizers of
CYP2D6 metabolized drugs (e.g., FLUox- INDICATIONS/ROUTES/DOSAGE
etine, PARoxetine). Pts predisposed to Note: May discontinue without tapering
hypotension. dose.

Canadian trade name Non-Crushable Drug High Alert drug


94 atorvaSTATin
A
Attention-Deficit Hyperactivity Disorder INTERVENTION/EVALUATION
(ADHD) Monitor urinary output; complaints of
PO: ADULTS, CHILDREN 6 YRS AND OLDER urinary retention/hesitancy may be a
WEIGHING 70 KG OR MORE: Initially, 40 mg related adverse reaction. Monitor B/P,
once daily. May increase after at least 3 days pulse periodically and following dose
to 80 mg daily. May further increase to 100 increases. Monitor for growth, attention
mg/day after 2-4 additional wks to achieve span, hyperactivity, unusual changes in
optimal response. Maximum: 100 mg. behavior, suicidal ideation. Assist with
CHILDREN 6 YRS AND OLDER WEIGHING LESS ambulation if dizziness occurs. Be alert
THAN 70 KG: Initially, 0.5 mg/kg/day. May to mood changes. Monitor fluid and
increase after at least 3 days to 1.2 mg/kg/ electrolyte status in pts with significant
day. Maximum: 1.4 mg/kg/day or 100 vomiting.
mg, whichever is less.
PATIENT/FAMILY TEACHING
Dosage in Hepatic Impairment
• Take last dose early in evening to
Expect to administer 50% of normal ato- avoid insomnia. • Report palpitations,
moxetine dosage to pts with moderate he- fever, vomiting, irritability. • Monitor
patic impairment and 25% of normal dos- growth rate, weight. • Report changes
age to pts with severe hepatic impairment. in behavior, suicidal ideation, chest pain,
Dosage in Renal Impairment palpitations, dyspnea.
No dose adjustment.
Dosage with Strong CYP2D6 Inhibitors atorvaSTATin
ADULTS: Initially, 40 mg/day. May in-
crease to 80 mg/day after minimum of 4 a-tor-va-sta-tin
wks. CHILDREN: Initially, 0.5 mg/kg/day. (Lipitor)
May increase to 1.2 mg/kg/day only after Do not confuse atorvastatin with
minimum 4-wk interval. atomoxetine, lovastatin, nys-
tatin, pitavastatin, pravastatin,
SIDE EFFECTS or simvastatin, or Lipitor with
Frequent: Headache, dyspepsia, nausea, Levatol, lisinopril, or Zocor.
vomiting, fatigue, decreased appetite,
­dizziness, altered mood. Occasional: Tachy- FIXED-COMBINATION(S)
cardia, hypertension, weight loss, delayed Caduet: atorvastatin/amLODIPine
growth in children, irritability. Rare: Insom- (calcium channel blocker): 10 mg/2.5
nia, sexual dysfunction in adults, fever. mg, 10 mg/5 mg, 10 mg/10 mg, 20
mg/2.5 mg, 20 mg/5 mg, 20 mg/10
ADVERSE EFFECTS/TOXIC mg, 40 mg/2.5 mg, 40 mg/5 mg, 40
REACTIONS mg/10 mg, 80 mg/5 mg, 80 mg/10 mg.
Urinary retention, urinary hesitancy may
occur. In overdose, gastric lavage, activated uCLASSIFICATION
charcoal may prevent systemic absorption. PHARMACOTHERAPEUTIC: Hy-
Severe hepatic injury occurs rarely. droxymethylglutaryl CoA (HMG-CoA)
­reductase inhibitor. CLINICAL: Anti-
NURSING CONSIDERATIONS hyperlipidemic.
BASELINE ASSESSMENT
Assess pulse, B/P before therapy, follow- USES
ing dose increases, and periodically dur-
Dyslipidemias: Primary prevention of
ing therapy. Assess attention span, inter-
cardiovascular disease in high-risk pts.
actions with others.
Reduces risk of stroke and heart attack

underlined – top prescribed drug


atorvaSTATin 95
A
in pts with type 2 diabetes with or without INTERACTIONS
evidence of heart disease. Reduces risk
of stroke in pts with or without evidence DRUG: Strong CYP3A4 inhibitors
of heart disease with multiple risk factors (e.g., clarithromycin, protease
other than diabetes. Adjunct to diet therapy inhibitors, itraconazole) may in-
in management of hyperlipidemias (re- crease concentration, risk of rhabdo-
duces elevations in total cholesterol, LDL-C, myolysis. CycloSPORINE may increase
apolipoprotein B, triglycerides in pts with concentration. Gemfibrozil, fibrates,
primary hypercholesterolemia), homozy- niacin, colchicine may increase risk
gous familial hypercholesterolemia, het- of myopathy, rhabdomyolysis. Strong
erozygous familial hypercholesterolemia CYP3A4 inducers (e.g., rifAMPin,
in pts 10–17 yrs of age, females more than efavirenz) may decrease concentration.
1 yr postmenarche. OFF-LABEL: Secondary HERBAL: St. John’s wort may decrease
prevention in pts who have experienced a level. FOOD: Grapefruit products may
noncardioembolic stroke/TIA or following increase serum concentrations. Red
an acute coronary syndrome (ACS) event. yeast rice may increase serum levels
(2.4 mg lovastatin per 600 mg rice). LAB
PRECAUTIONS VALUES: May increase serum transami-
Contraindications: Hypersensitivity to nase, creatinine kinase concentrations.
atorvastatin. Active hepatic disease, breast-
feeding, pregnancy or women who may be-
AVAILABILITY (Rx)
come pregnant, unexplained elevated LFT Tablets: 10 mg, 20 mg, 40 mg, 80 mg.
results. Cautions: Anticoagulant therapy;
history of hepatic disease; substantial alco- ADMINISTRATION/HANDLING
hol consumption; pts with prior stroke/TIA; PO
concomitant use of potent CYP3A4 inhibi- • Give without regard to food or time of
tors; elderly (predisposed to myopathy). day. • Do not break, crush, dissolve, or
divide film-coated tablets.
ACTION
Inhibits HMG-CoA reductase, the enzyme INDICATIONS/ROUTES/DOSAGE
that catalyzes the early step in cholesterol Do not use in pts with active hepatic dis-
synthesis. Results in an increase of ex- ease.
pression in LDL receptors on hepatocyte Note: Individualize dosage based on
membranes and a stimulation of LDL baseline LDL/cholesterol, goal of ther-
catabolism. Therapeutic Effect: De- apy, pt response. Maximum dose with
creases LDL and VLDL, plasma triglycer- strong CYP3A4 inhibitors: 20 mg/day.
ide levels; increases HDL concentration.
Dyslipidemias
PHARMACOKINETICS PO: ADULTS, ELDERLY: Initially, 10–20
Poorly absorbed from GI tract. Protein mg/day (40 mg in pts requiring greater
binding: greater than 98%. Metabolized than 45% reduction in LDL-C). Range:
in liver. Primarily excreted in feces (bili- 10–80 mg/day.
ary). Half-life: 14 hrs. Heterozygous Hypercholesterolemia
PO: CHILDREN 10–17 YRS: Initially, 10
LIFESPAN CONSIDERATIONS mg/day. Maximum: 20 mg/day.
Pregnancy/Lactation: Distributed in
breast milk. Contraindicated during preg- Dosage in Renal Impairment
nancy. May produce fetal skeletal malfor- No dose adjustment.
mation. Children: Safety and efficacy
Dosage in Hepatic Impairment
not established. Elderly: No age-related
See contraindications.
precautions noted.

Canadian trade name Non-Crushable Drug High Alert drug


96 avelumab
A
SIDE EFFECTS USES
Common: Atorvastatin is generally well Treatment of adults and pediatric pts
tolerated. Side effects are usually mild 12 yrs and older with metastatic Merkel
and transient. Frequent (16%): Headache. cell carcinoma. Treatment of pts with lo-
Occasional (5%–2%): Myalgia, rash, pru- cally advanced or metastatic urothelial
ritus, allergy. Rare (less than 2%–1%): carcinoma who have disease progres-
Flatulence, dyspepsia, depression. sion during or following platinum-­
containing chemotherapy or have disease
ADVERSE EFFECTS/TOXIC ­progression within 12 mos of neoadju-
REACTIONS vant or adjuvant treatment with platinum-
Potential for cataracts, photosensitivity, containing chemotherapy. First-line treat-
myalgia, rhabdomyolysis. ment of advanced renal cell carcinoma
(in combination with axitinib).
NURSING CONSIDERATIONS
PRECAUTIONS
BASELINE ASSESSMENT Contraindications: Hypersensitivity to
Obtain baseline cholesterol, triglycerides, avelumab. Cautions: Acute infection, con-
LFT. Question for possibility of pregnancy be- ditions predisposing to infection (e.g.,
fore initiating therapy. Obtain dietary history. diabetes, immunocompromised pts, renal
INTERVENTION/EVALUATION
failure, open wounds); corticosteroid in-
tolerance, hematologic cytopenias, hepatic
Monitor for headache. Assess for rash, impairment, interstitial lung disease, renal
pruritus, malaise. Monitor cholesterol, insufficiency; history of autoimmune dis-
triglyceride lab values for therapeutic re- orders (Crohn’s disease, demyelinating
sponse. Monitor LFTs, CPK. polyneuropathy, Guillain-Barré syndrome,
PATIENT/FAMILY TEACHING Hashimoto’s thyroiditis, hyperthyroidism,
• Follow special diet (important part of myasthenia gravis, rheumatoid arthritis,
treatment). • Periodic lab tests are es- Type I diabetes, vasculitis); CVA, diabetes,
sential part of therapy. • Do not take intestinal obstruction, pancreatitis.
other medications without consulting ACTION
physician. • Do not chew, crush, dis-
solve, or divide tablets. • Report dark Binds to PD-L1 and blocks interaction with
urine, muscle fatigue, bone pain. both PD-L1 and B7.1 receptors while still
• Avoid excessive alcohol intake, large allowing interaction between PD-L2 and PD-
quantities of grapefruit products. L1. PD-L1 is an immune check point protein
expressed on tumor cells, down regulating
anti-tumor T-cell function. Therapeutic
avelumab Effect: Restores immune responses, in-
cluding T-cell anti-tumor function.
a-vel-ue-mab PHARMACOKINETICS
(Bavencio)
Do not confuse avelumab with Widely distributed. Degraded into small
durvalumab, nivolumab or peptides and amino acids via proteo-
olaratumab. lytic enzymes. Steady state reached in
4–6 wks. Excretion not specified. Half-
uCLASSIFICATION life: 6.1 days.
PHARMACOTHERAPEUTIC: Pro- LIFESPAN CONSIDERATIONS
grammed death ligand-1 (PD-L1)
blocking antibody. Monoclonal antibody. Pregnancy/Lactation: Avoid pregnancy;
CLINICAL: Antineoplastic. may cause fetal harm. Females of re-
productive potential should use effective
underlined – top prescribed drug
avelumab 97
A
contraception during treatment and for IV INCOMPATIBILITIES
at least 1 mo after discontinuation. Un- Do not mix or infuse with other medica-
known if distributed in breast milk. How- tions.
ever, human immunoglobulin G (IgG)
is present in breast milk and is known INDICATIONS/ROUTES/
to cross the placenta. Breastfeeding not DOSAGE
recommended during treatment and for Note: Premedicate with acetaminophen
at least 1 mo after discontinuation. Chil- and an antihistamine prior to the first 4
dren: Safety and efficacy not established infusions. Consider premedication for
in pts younger than 12 yrs. Elderly: No subsequent infusions based on prior in-
age-related precautions noted. fusion reactions.
INTERACTIONS Urothelial Carcinoma, Merkel Cell
DRUG: May enhance adverse effects/toxic- Carcinoma
ity of belimumab. HERBAL: None signifi- IV: ADULTS, ELDERLY, CHILDREN:10 mg/kg
cant. FOOD: None known. LAB VALUES: every 2 wks. Continue until disease pro-
May decrease Hgb, Hct, lymphocytes, gression or unacceptable toxicity.
neutrophils, platelets, RBCs. May increase
serum alkaline phosphatase, ALT, AST, Renal Cell Carcinoma (Advanced)
amylase, bilirubin, glucose, GGT, lipase. IV: ADULTS, ELDERLY: 800 mg once q2wks
or 10 mg/kg q2wks (in combination with
AVAILABILITY (Rx) axitinib) until disease progression or unac-
Injection: 200 mg/10 mL (20 mg/mL). ceptable toxicity.

ADMINISTRATION/HANDLING Dose Modification


Infusion-Related Reactions
IV CTCAE Grade 1 or 2: Interrupt or de-
Preparation • Visually inspect for crease rate of infusion. CTCAE Grade 3
particulate matter or discoloration. Solu- or 4: Permanently discontinue.
tion should appear clear and colorless to Endocrinopathies (e.g., Adrenal
slightly yellow in color. • Do not use if Insufficiency, Hyperglycemia,
solution is cloudy, discolored, or if visi- Hyperthyroidism, Hypothyroidism)
ble particles are observed. • Withdraw (Treatment-Induced)
proper volume from vial and inject into a CTCAE Grade 3 or 4 endocrinopa-
250-mL bag of 0.9% NaCl or 0.45% thies: Withhold treatment until resolved
NaCl. • Gently invert to mix; avoid to Grade 1 or 0, then resume therapy
foaming. • Do not shake. • Diluted after corticosteroid taper. Consider hor-
solution should be clear, colorless, and mone replacement therapy if hypothy-
free of particles. roidism ­occurs.
Rate of administration • Infuse over
60 min via dedicated IV line using a ster- Colitis (Treatment-Induced)
ile, nonpyrogenic, low protein-binding CTCAE Grade 2 or 3 diarrhea or coli-
in-line filter. tis: Withhold treatment until resolved to
Storage • Refrigerate unused vi- Grade 1 or 0, then resume therapy after cor-
als. • May refrigerate diluted solution ticosteroid taper. CTCAE Grade 4 diar-
for no more than 24 hrs or store at room rhea or colitis; recurrent Grade 3 diar-
temperature for no more than 4 hrs. If rhea or colitis: Permanently ­discontinue.
refrigerated, allow diluted solution to
warm to room temperature before infus- Hepatitis (Treatment-Induced)
ing. • Do not freeze or shake. • Pro- Serum ALT/AST greater than
tect from light. 3 and up to 5 times upper limit

Canadian trade name Non-Crushable Drug High Alert drug


98 avelumab
A
normal (ULN) or serum bilirubin SIDE EFFECTS
greater than 1.5 and up to 3 times
Note: Percentage of side effects may vary
ULN): Withhold treatment until resolved
depending on indication of treatment.
to Grade 1 or 0, then resume therapy. Se- Frequent (50%–18%): Fatigue, muscu-
rum ALT/AST greater than 5 times
loskeletal pain, diarrhea, rash, infusion
upper limit normal (ULN) or se-
reactions (back pain, chills, pyrexia, hypo-
rum bilirubin greater than 3 times
tension), nausea, decreased appetite, pe-
ULN): Permanently ­discontinue.
ripheral edema, cough. Occasional (17%–
Nephritis and Renal Dysfunction 10%): Constipation, arthralgia, abdominal
(Treatment-Induced) pain, decreased weight, dizziness, vomiting,
Serum creatinine greater than 1.5 hypertension, dyspnea, pruritus, headache.
and up to 6 times ULN: Withhold
treatment until resolved to Grade 1 or 0,
ADVERSE EFFECTS/TOXIC
then resume therapy after corticosteroid
REACTIONS
taper. Serum creatinine greater than Anemia, neutropenia, thrombocytope-
6 times ULN: Permanently ­discontinue. nia is an expected response to therapy.
Other moderate or severe symptoms May cause severe, sometimes fatal cases
of treatment-induced reactions (e.g., of immune-mediated reactions such as
arthritis, bullous dermatitis, encepha- pneumonitis (1% of pts), hepatitis (1%
litis, erythema multiform, exfoliative of pts), colitis (2% of pts), adrenal insuf-
dermatitis, demyelination, Guillain- ficiency (1% of pts), hypothyroidism, hy-
Barré syndrome, hemolytic anemia, perthyroidism (6% of pts), type 1 diabetes
histiocytic necrotizing lymphadenitis, mellitus including ketoacidosis (less than
hypophysitis, hypopituitarism, iritis, 1% of pts), nephritis (less than 1% of pts),
myasthenia gravis, myocarditis, my- other immune-mediated effects (less than
ositis, pancreatitis, pemphigoid, pso- 1%). Cellulitis, CVA, dyspnea, ileus, peri-
riasis, Stevens Johnson Syndrome/ cardial effusion, small bowel/intestinal ob-
toxic epidermal necrolysis, rhabdo- struction, renal failure, respiratory failure,
myolysis, uveitis, vasculitis): Withhold septic shock, transaminitis, urosepsis may
treatment until resolved to Grade 1 or 0, occur. Immunogenicity (auto-avelumab
then resume therapy after corticosteroid antibodies) reported in 4% of pts.
taper. Life-threatening adverse effects,
recurrent severe immune-mediated
NURSING CONSIDERATIONS
reactions; requirement of predni- BASELINE ASSESSMENT
SONE 10 mg/day or greater (or equiv- Obtain ANC, CBC, BMP (esp. serum cre-
alent) for more than 2 wks; persistent atinine, creatinine clearance; BUN), TSH,
Grade 2 or 3 immune-mediated reac- vital signs; urine pregnancy. Question
tion lasting 12 wks or longer: Perma- current breastfeeding status. Verify use of
nently discontinue. contraception in female pts of reproduc-
Pneumonitis (Treatment-Induced) tive potential. Question history of prior
CTCAE Grade 2 pneumonitis: With- hypersensitivity reaction, infusion-related
hold treatment until resolved to Grade 1 reactions, allergy to corticosteroids/pred-
or 0, then resume therapy after cortico- nisone. Screen for history of autoimmune
steroid taper. CTCAE Grade 3 or 4 or disorders, diabetes, pituitary/pulmonary/
recurrent Grade 2 pneumonitis: Per- thyroid disease, renal insufficiency. Obtain
manently discontinue. nutrition consult. Offer emotional support.
INTERVENTION/EVALUATION
Dosage in Renal/Hepatic Impairment
Not specified; use caution. Monitor ANC, CBC, BMP, creatinine clear-
ance, thyroid panel (if applicable); vital

underlined – top prescribed drug


axitinib 99
A
signs. Diligently monitor for infusion-
related reactions, treatment-related axitinib
toxicities, esp. during initial infusions.
If immune-mediated reactions occur, ax-i-ti-nib
consider referral to specialist; pt may (Inlyta)
require treatment with corticosteroids. Do not confuse axitinib with
Screen for allergic reactions, acute infec- afatinib, ibrutinib, or imatinib.
tions (cellulitis, sepsis, UTI), hepatitis,
uCLASSIFICATION
pulmonary events (dyspnea, pneumo-
nitis, pneumonia). Monitor strict I&O, PHARMACOTHERAPEUTIC: Vascular
hydration status, stool frequency and endothelial growth factor (VEGF)
consistency. Encourage proper calorie inhibitor. Tyrosine kinase inhibitor.
intake and nutrition. Assess skin for rash, CLINICAL: Antineoplastic.
lesions, dermal toxicities.
PATIENT/FAMILY TEACHING USES
• Treatment may depress your immune Treatment of advanced renal cell carci-
system and reduce your ability to fight in- noma after failure of one prior systemic
fection. Report symptoms of infection such chemotherapy.
as body aches, burning with urination,
chills, cough, fatigue, fever. Avoid those PRECAUTIONS
with active infection. • Avoid pregnancy; Contraindications: Hypersensitivity to
treatment may cause birth defects. Do not axitinib. Cautions: Pts with increased
breastfeed. Females of childbearing poten- risk or history of thrombotic events
tial should use effective contraception dur- (CVA, MI), GI perforation or fistula
ing treatment and for at least 1 mo after formation, renal/hepatic impairment,
discontinuation. • Serious adverse reac- hypertension, HF. Do not use in pts with
tions may affect lungs, liver, intestines, untreated brain metastasis or recent ac-
kidneys, hormonal glands, nervous system, tive GI bleeding.
which may require anti-inflammatory med-
ication. • Immediately report any serious ACTION
or life-threatening inflammatory symptoms Inhibits vascular endothelial growth factor
in the following body systems: colon (se- receptors. Therapeutic Effect: Blocks
vere abdominal pain/swelling, diarrhea); tumor growth, inhibits angiogenesis.
kidneys (decreased or dark-colored urine,
flank pain); lung (chest pain, severe PHARMACOKINETICS
cough, shortness of breath); liver (bruis- Metabolized in liver. Protein binding:
ing, dark-colored urine, clay-colored/tarry greater than 99%. Excreted primarily in
stools, nausea, yellowing of the skin or feces with a lesser amount excreted in
eyes); nervous system (paralysis, weak- urine. Half-life: 2.5–6 hrs.
ness); pituitary (persistent or unusual
headaches, dizziness, extreme weakness, LIFESPAN CONSIDERATIONS
fainting, vision changes); skin (blisters, Pregnancy/Lactation: May cause fetal
bubbling, inflammation, rash); thyroid harm. Unknown whether distributed in
(trouble sleeping, high blood pressure, breast milk. Children: Safety and ef-
fast heart rate [overactive thyroid]; fatigue, ficacy not established. Elderly: No age-
goiter, weight gain [underactive thyroid]); related precautions noted.
vascular (low blood pressure, vein/artery
pain or irritation). • Do not take any INTERACTIONS
over-the-counter anti-inflammatory medi- DRUG: Strong CYP3A4/5 inhibitors
cations unless approved by your doctor. (e.g., erythromycin, ketoconazole,

Canadian trade name Non-Crushable Drug High Alert drug


100 axitinib
A
ritonavir) may significantly increase con- SIDE EFFECTS
centration; do not use concurrently. If used, Frequent (55%–20%): Diarrhea, hyper-
reduce dose by 50%. Coadministration tension, fatigue, decreased appetite, nau-
with strong CYP3A4/5 inducers (e.g., sea, dysphonia, palmar-plantar eryth-
rifAMPin, phenytoin, carBAMaze- rodysesthesia (hand-foot) syndrome,
pine, PHENobarbital) may significantly weight loss, vomiting, asthenia, consti-
decrease concentration; do not use con- pation. Occasional (19%–11%): Hypo-
currently. HERBAL: St. John’s wort may thyroidism, cough, stomatitis, arthral-
decrease concentration. FOOD: Grape- gia, dyspnea, abdominal pain, headache,
fruit products may increase concentra- peripheral pain, rash, proteinuria,
tion. LAB VALUES: May decrease Hgb, dysgeusia. Rare (10%–2%): Dry skin,
WBC count, platelets, lymphocytes; serum dyspepsia, dizziness, myalgia, pruritus,
calcium, alkaline phosphatase, albumin, epistaxis, alopecia, hemorrhoids, tinni-
sodium, phosphate, b­ icarbonate. May in- tus, erythema.
crease serum ALT, AST, bilirubin, BUN, cre-
atinine, serum potassium, lipase, amylase; ADVERSE EFFECTS/TOXIC
urine protein. May alter serum glucose. REACTIONS
Arterial and venous thrombotic events
AVAILABILITY (Rx)
(MI, CVA), GI perforation, fistula, hemor-
Tablets, Film-Coated: 1 mg, 5 mg. rhagic events (including cerebral hemor-
rhage, hematuria, hemoptysis, GI bleed-
ADMINISTRATION/HANDLING ing), hypertensive crisis, cardiac failure
PO have been observed and can be fatal. Hy-
• Give without regard to food. • Swal- pothyroidism requiring thyroid hormone
low tablets whole with full glass of water. replacement has been noted. ­Reversible
­posterior ­leukoencephalopathy syn-
INDICATIONS/ROUTES/DOSAGE drome (RPLS) has been observed.
Renal Cell Carcinoma
PO: ADULTS, ELDERLY: Initially, 5 mg twice NURSING CONSIDERATIONS
daily, given approximately 12 hrs apart. If BASELINE ASSESSMENT
tolerated (no adverse events above Grade
2, B/P normal, and no antihypertension Obtain baseline BMP, LFT, renal func-
use for at least 2 consecutive wks), may in- tion test, urine protein, serum amylase,
crease to 7 mg twice daily, then 10 mg twice lipase, phosphate before initiation of,
daily. For adverse effects, may decrease to and periodically throughout, treatment.
3 mg twice daily, then 2 mg twice daily if Offer emotional support. Assess medi-
adverse effects persist. cal history, esp. hepatic function abnor-
malities. B/P should be well controlled
Dose Modification prior to initiating treatment. Stop medi-
Dosage with concomitant strong cation at least 24 hrs prior to sched-
CYP3A4 inhibitors: Reduce dose uled surgery. Monitor thyroid function
by 50%. (Avoid concomitant use if before and periodically throughout
­possible.) treatment.
Dosage in Renal Impairment INTERVENTION/EVALUATION
No dose adjustment. Use caution in ESRD. Monitor CBC, BMP, LFT, renal function
test, urine protein, serum amylase, li-
Dosage in Hepatic Impairment
pase, phosphate, thyroid tests. Monitor
Mild impairment: No dose adjustment.
daily pattern of bowel activity, stool con-
Moderate impairment: Reduce initial
sistency. Assess for evidence of bleeding
dose by 50%. Severe impairment: Not or hemorrhage. Assess for hypertension.
recommended.
underlined – top prescribed drug
azaTHIOprine 101
A
For persistent hypertension despite use reduction of steroid use in Crohn’s dis-
of antihypertensive medications, dose ease, lupus nephritis, chronic refractory
should be reduced. Permanently discon- immune thrombocytopenic purpura.
tinue if signs or symptoms of RPLS occur
(extreme lethargy, increased B/P from PRECAUTIONS
pt baseline, pyuria). Contact physician if Contraindications: Hypersensitivity to
changes in voice, redness of skin, or rash azaTHIOprine. Pregnant women with RA,
is noted. pts previously treated for RA with alkylat-
PATIENT/FAMILY TEACHING ing agents (cyclophosphamide, chloram-
• Avoid crowds, those with known in- bucil, melphalan) may have a prohibitive
fection. • Avoid contact with anyone risk of malignancy with azathioprine.
Cautions: Immunosuppressed pts, pts
who recently received live virus vaccine;
do not receive vaccinations. • Swal- with hepatic/renal impairment, active
low tablet whole; do not chew, crush, infection. Testing for genetic deficiency
dissolve, or divide. • Avoid grapefruit of thiopurine methyltransferase should
products. • Report persistent diar- be obtained. (Absence or ­reduced levels
rhea, extreme fatigue, abdominal pain, increase risk of myelosuppression.)
yellowing of skin or eyes, bruising eas- PHARMACOKINETICS
ily; bleeding of any kind, esp. bloody
stool or urine; confusion, seizure activ- Well absorbed from GI tract. Peak levels:
ity, vision loss, trouble speaking, chest 1–2 hrs. Protein binding: 30%. Metabo-
pain; difficulty breathing, leg pain or lized in liver. Primarily excreted in urine.
swelling. Half-life: 2 hrs.

ACTION
azaTHIOprine Metabolites are incorporated into repli-
cating DNA and halt replication. Blocks
a-za-thy-o-preen purine synthesis pathway. Therapeutic
(Azasan, Imuran) Effect: Suppresses cell-mediated hy-
persensitivities; alters antibody produc-
j BLACK BOX ALERT j Chronic tion, immune response in transplant
immunosuppression increases risk
of developing malignancy. recipients. Reduces symptoms of arthritis
Do not confuse azaTHIOprine severity.
with Azulfidine, azaCITIDine, or
azithromycin, or Imuran with LIFESPAN CONSIDERATIONS
Elmiron, Imdur, or Inderal. Pregnancy/Lactation: May depress
spermatogenesis, reduce sperm viabil-
uCLASSIFICATION ity, count. May cause fetal harm. Do not
PHARMACOTHERAPEUTIC: Immu- breastfeed. Children: Safety and efficacy
nologic agent. CLINICAL: Immuno- not established. Elderly: No age-related
suppressant. precautions noted.
INTERACTIONS
USES DRUG: Allopurinol may increase ac-
Adjunct in prevention of rejection in tivity, toxicity. May increase immunosup-
kidney transplantation. Treatment of pressive effect of baricitinib, fingoli-
rheumatoid arthritis (RA) in pts unre- mod, mercaptopurine. May decrease
sponsive to conventional therapy. OFF- the therapeutic effect of BCG (intra-
LABEL: Treatment of dermatomyositis, vesical), vaccines (live). May in-
polymyositis. Maintenance, remission, or crease adverse effects of natalizumab,

Canadian trade name Non-Crushable Drug High Alert drug


102 azaTHIOprine
A
vaccines (live). HERBAL: Echina- Creatinine
cea may diminish therapeutic effect. Clearance Dosage
FOOD: None known. LAB VALUES: May Hemodialysis 50% of normal (Adults:
decrease Hgb, serum albumin, uric additional 0.25 mg/kg)
acid, leukocytes, platelet count. May Continuous re- 75% of normal
increase serum ALT, AST, alkaline nal replace-
phosphatase, amylase, bilirubin. ment therapy
(CRRT)
AVAILABILITY (Rx)
Tablets: (Imuran): 50 mg, (Azasan): 75 Dosage in Hepatic Impairment
mg, 100 mg. No dose adjustment.
ADMINISTRATION/HANDLING SIDE EFFECTS
PO Frequent: Nausea, vomiting, anorexia (par-
• Give with food or in divided doses to ticularly during early treatment and with
reduce potential for GI disturbances. large doses). Occasional: Rash. Rare: Se-
• Store oral form at room temperature. vere nausea/vomiting with diarrhea, ab-
dominal pain, hypersensitivity reaction.
INDICATIONS/ROUTES/
DOSAGE ADVERSE EFFECTS/
b ALERT c Reduce dose to 1/3 or 1/4 TOXIC REACTIONS
usual dose when used with allopurinol or Increases risk of neoplasia (new
in low/absent thiopurine methyltransfer- abnormal-growth tumors). Significant
­
ase genetic deficiency. leuko­penia and thrombocytopenia may
Prevention of Renal Allograft Rejection
occur, particularly in pts undergoing re-
PO: ADULTS, ELDERLY, CHILDREN: 3–5 mg/
nal transplant rejection. Hepatotoxicity
kg/day on day of transplant (or 1–3 days occurs rarely.
prior to transplant), then 1–3 mg/kg/day
as maintenance dose. NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Rheumatoid Arthritis (RA)
PO: ADULTS, ELDERLY: Initially, 1 mg/kg/ Arthritis: Assess onset, type, location,
day (50–100 mg) as a single dose or in and duration of pain, fever, inflamma-
2 divided doses for 6–8 wks. May tion. Inspect appearance of affected
increase by 0.5 mg/kg/day after 6–8 wks joints for immobility, deformities, skin
at 4-wk intervals. Maximum: 2.5 mg/ condition.
kg/day. Maintenance: Lowest effective INTERVENTION/EVALUATION
dosage. May decrease dose by 0.5 mg/kg CBC, LFT should be performed weekly
or 25 mg/day q4wks (while other thera- during first mo of therapy, twice
pies, such as rest, physiotherapy, and monthly during second and third mos
salicylates, are maintained). May discon- of treatment, then monthly thereafter.
tinue abruptly. If WBC falls rapidly, dosage should be
Dosage in Renal Impairment reduced or discontinued. Assess par-
Dosage is modified based on creatinine ticularly for delayed myelosuppression.
clearance. Routinely watch for any change from
baseline. Arthritis: Assess for thera-
Creatinine
peutic response: relief of pain, stiff-
Clearance Dosage
ness, swelling; increased joint mobility;
10–50 mL/min 75% of normal reduced joint tenderness; improved
Less than 50% of normal
10 mL/min
grip strength.

underlined – top prescribed drug


azilsartan 103
A
PATIENT/FAMILY TEACHING decreases peripheral resistance, de-
• Contact physician if unusual bleeding/ creases B/P.
bruising, sore throat, mouth sores, ab-
dominal pain, fever occurs. • Thera- PHARMACOKINETICS
peutic response in rheumatoid arthritis Hydrolyzed to active metabolite in GI
may take up to 12 wks. • Women of tract. Moderately absorbed (60%). Peak
childbearing age must avoid pregnancy. plasma concentration: 1.5–3 hrs. Metab-
olized in liver. Protein binding: greater
than 99%. Excreted in feces (55%), urine
azilsartan (42%). Half-life: 11 hrs.

a-zil-sar-tan LIFESPAN CONSIDERATIONS


(Edarbi) Pregnancy/Lactation: May cause
j BLACK BOX ALERT jMay fetal harm when administered during
cause fetal injury, mortality. Dis- third trimester. Unknown if distributed
continue as soon as possible once in breast milk. Breastfeeding not rec-
pregnancy is detected. ommended. Children: Safety and effi-
Do not confuse azilsartan with cacy not e­ stablished. Elderly: Elevated
losartan, irbesartan, or valsartan. creatinine levels may occur in pts older
than 75 yrs.
FIXED-COMBINATION(S)
Edarbyclor: azilsartan/chlorthali- INTERACTIONS
done, a diuretic: 40 mg/12.5 mg, 40 DRUG: ACE inhibitors (e.g., enala-
mg/25 mg. pril, lisinopril), potassium-sparing
uCLASSIFICATION
diuretics (e.g., spironolactone, tri-
amterene), potassium supplements
PHARMACOTHERAPEUTIC: Angio- may increase risk of hyperkalemia.
tensin II receptor blocker (ARB). NSAIDs, COX-2 inhibitors (e.g., ce-
CLINICAL: Antihypertensive. lecoxib) may decrease effect. Hypoten-
sive agents may increase hypotensive
USES effects. May increase concentration/effect
Treatment of hypertension alone or in of lithium. HERBAL: Herbals with hy-
combination with other antihypertensives. pertensive properties (e.g., licorice,
yohimbe) or hypotensive properties
PRECAUTIONS (e.g., garlic, ginger, ginkgo biloba)
Contraindications: Hypersensitivity to may alter effects. FOOD: None known.
azilsartan. Concomitant use with aliski- LAB VALUES: May increase serum creati-
ren in pts with diabetes. Cautions: Re- nine. May decrease Hgb, Hct.
nal/hepatic impairment, unstented
renal artery stenosis, significant aor- AVAILABILITY (Rx)
tic/mitral stenosis, severe HF, volume Tablets: 40 mg, 80 mg.
depletion/salt-depleted pts, history of
angioedema. ADMINISTRATION/HANDLING
PO
ACTION • May give without regard to food.
Inhibits vasoconstriction, aldosterone-
secreting effects of angiotensin II, INDICATIONS/ROUTES/DOSAGE
blocking the binding of angiotensin Hypertension
II to AT1 receptors in vascular smooth PO: ADULTS, ELDERLY: Initially, 40 mg
muscle and adrenal gland tissue. Ther- once daily. May increase up to 80 mg
apeutic Effect: Produces vasodilation, once daily.

Canadian trade name Non-Crushable Drug High Alert drug


104 azithromycin
A
Dosage in Renal/Hepatic Impairment
No dose adjustment. azithromycin
SIDE EFFECTS a-zith-roe-mye-sin
Occasional (2%–0.4%): Diarrhea, ortho- (AzaSite, Zithromax SR, Zithromax
static hypotension. Rare (0.3%): Nausea, TRI-PAK, Zithromax Z-PAK)
fatigue, muscle spasm, cough. Do not confuse azithromycin
with azaTHIOprine or eryth-
ADVERSE EFFECTS/TOXIC romycin, or Zithromax with
REACTIONS Fosamax or Zovirax.
Oliguria, acute renal failure may occur in
uCLASSIFICATION
pts with history of renal artery stenosis,
severe HF, volume depletion. PHARMACOTHERAPEUTIC: Mac-
rolide. CLINICAL: Antibiotic.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT USES
Obtain baseline Hgb, Hct, BMP, LFT. Ob- IV/PO: Treatment of susceptible infec-
tain B/P, apical pulse immediately before tions due to Chlamydia pneumoniae,
each dose, in addition to regular moni- C. trachomatis, H. influenzae, Legio­
toring (be alert to fluctuations). Question nella, M. catarrhalis, Mycoplasma pneu­
for possibility of pregnancy. Assess medi- moniae, N. gonorrhoeae, S. aureus.,
cation history (esp. diuretics). Question S. pneumoniae, S. pyogenes, including
history of hepatic/renal impairment, re- mild to moderate infections of upper re-
nal artery stenosis, severe HF. spiratory tract (pharyngitis, tonsillitis),
lower respiratory tract (acute bacterial
INTERVENTION/EVALUATION exacerbations, COPD, pneumonia), un­
Maintain hydration (offer fluids fre- complicated skin and skin-structure in-
quently). Monitor serum electrolytes, fections, sexually transmitted diseases
B/P, pulse, hepatic/renal function. (nongonococcal urethritis, cervicitis due
­Observe for symptoms of hypotension. to C. trachomatis), chancroid. Prevents
If excessive reduction in B/P occurs, ­disseminated Mycobacterium avium
place pt in supine position, feet slightly complex (MAC). Treatment of mycoplasma
elevated. Correct volume or salt depletion pneumonia, community-acquired pneu-
prior to treatment. monia, pelvic inflammatory disease (PID).
Prevention/treatment of MAC in pts with
PATIENT/FAMILY TEACHING advanced HIV infection. OFF-LABEL: Prophy-
laxis of endocarditis. Prevention of pulmo-
• Take measures to avoid pregnancy. If
nary exacerbations in pts with cystic fibrosis.
pregnancy occurs, inform physician im-
Ophthalmic: Treatment of bacterial con-
mediately. • Low blood pressure is
junctivitis caused by susceptible infections
more likely to occur if pt takes diuretics
due to H. influenzae, S. aureus, S. mitis,
or other medications to control hyper-
S. pneumoniae. Prevention of pulmonary
tension, consumes low-salt diet, experi-
exacerbations in pts with cystic fibrosis.
ences vomiting or diarrhea, or becomes
dehydrated. • Change positions slowly, PRECAUTIONS
particularly from lying to standing posi- Contraindications:Hypersensitivity to
tion. • Report light-headedness or diz- azithromycin, erythromycin, or other
ziness; lie down immediately. • Report macrolide antibiotics. History of chole-
swollen extremities or decreased urine static jaundice/hepatic impairment as-
output despite fluid intake. sociated with prior azithromycin therapy.

underlined – top prescribed drug


azithromycin 105
A
­ autions: Hepatic/renal impairment, myas-
C ADMINISTRATION/HANDLING
thenia gravis, hepatocellular and/or chole-
static hepatitis (with or without jaundice), IV
hepatic necrosis. May prolong QT interval. Reconstitution • Reconstitute each
500-mg vial with 4.8 mL Sterile Water
ACTION
for Injection to provide concentration of
Binds to ribosomal receptor sites of 100 mg/mL. • Shake well to ensure
susceptible organisms, inhibiting RNA-­ dissolution. • Further dilute with 250
dependent protein synthesis. Therapeutic or 500 mL 0.9% NaCl or D5W to provide
Effect: Bacteriostatic or bactericidal, de- final concentration of 2 mg/mL with 250
pending on drug dosage. mL diluent or 1 mg/mL with 500 mL di-
PHARMACOKINETICS luent.
Rate of administration • Infuse over
Rapidly absorbed from GI tract. Protein 60 min (2 mg/mL). Infuse over 3 hrs (1
binding: 7%–50%. Widely distributed. mg/mL).
Metabolized in liver. Excreted primarily Storage • Store vials at room tem-
by biliary excretion. Half-life: 68 hrs. perature. • Following reconstitution,
LIFESPAN CONSIDERATIONS diluted solution is stable for 24 hrs at
room temperature or 7 days if refriger-
Pregnancy/Lactation: Unknown
ated.
if distributed in breast milk. Chil-
dren: Safety and efficacy not established PO
in pts younger than 16 yrs for IV use • Give without regard to food. • May
and younger than 6 mos for oral use. store suspension at room temperature.
Elderly: No age-related precautions in Stable for 10 days after reconstitution.
those with normal renal function.
Ophthalmic
INTERACTIONS • Place gloved finger on lower eyelid
DRUG: Aluminum/magnesium-con- and pull out until a pocket is formed be-
taining antacids may decrease concen- tween eye and lower lid. • Place pre-
tration (give 1 hr before or 2 hrs after scribed number of drops into
antacid). May increase concentration/ pocket. • Instruct pt to close eye gently
effect of amiodarone, colchicine, cy- for 1 to 2 min (so that medication will
cloSPORINE, dabigatran, dronedar- not be squeezed out of sac) and to apply
one, edoxaban, pazopanib, QT-pro- digital pressure to lacrimal sac at inner
longing medications, thioridazine, canthus for 1 min to minimize systemic
topotecan, toremifene, ziprasidone. absorption.
QUEtiapine may increase concentration.
HERBAL: None significant. FOOD: None IV INCOMPATIBILITIES
known. LAB VALUES: May increase se- CefTRIAXone (Rocephin), ciprofloxacin
rum creatine phosphokinase (CPK), ALT, (Cipro), famotidine (Pepcid), furo-
AST, bilirubin, LDH, potassium. semide (Lasix), ketorolac (Toradol),
levoFLOXacin (Levaquin), morphine,
AVAILABILITY (Rx) piperacillin/tazobactam (Zosyn), potas-
Injection, Powder for Reconstitution: (Zith- sium chloride.
romax): 500 mg. Ophthalmic Solution:
(AzaSite): 1%. Packet, Oral: 1g. Suspen-
IV COMPATIBILITIES
sion, Oral: (Zithromax): 100 mg/5 mL, Ceftaroline (Teflaro), doripenem (Doribax),
200 mg/5 mL. Tablets: 250 mg, 500 mg, ondansetron (Zofran), tigecycline (Tygacil),
600 mg. diphenhydrAMINE (Benadryl).

Canadian trade name Non-Crushable Drug High Alert drug


106 azithromycin
A
INDICATIONS/ROUTES/DOSAGE complete course of therapy. CHILDREN 6
Usual Dosage Range MOS–15 YRS: 10 mg/kg on day 1 (maxi-
PO: ADULTS, ELDERLY: 250–600 mg once mum: 500 mg), then 5 mg/kg (maxi-
daily or 1–2 g as single dose. CHILDREN mum: 250 mg) on days 2–5.
6 MOS AND OLDER: 5–12 mg/kg (maxi-
Bacterial Conjunctivitis
mum: 500 mg) once daily or 30 mg/kg Ophthalmic: ADULTS, ELDERLY: 1 drop
(maximum: 1,500 mg) as single dose. in affected eye twice daily for 2 days, then
(Zmax): 60 mg/kg as a single dose. 1 drop once daily for 5 days.
­ EONATES: 10–20 mg/kg once daily.
N
IV: ADULTS, ELDERLY: 250–500 mg once Dosage in Renal/Hepatic Impairment
daily CHILDREN, NEONATES: 10 mg/kg Use caution.
once daily.
SIDE EFFECTS
Mild to Moderate Respiratory Tract, Skin,
Occasional: Systemic: Nausea, vomiting,
Soft Tissue Infections
diarrhea, abdominal pain. Ophthalmic:
PO: ADULTS, ELDERLY: 500 mg day 1,
Eye irritation. Rare: Systemic: Headache,
then 250 mg days 2–5.
dizziness, allergic reaction.
MAC Prevention
PO: ADULTS, ELDERLY, ADOLESCENTS:
ADVERSE EFFECTS/TOXIC
1,200 mg once weekly or 600 mg twice REACTIONS
weekly. CHILDREN: 20 mg/kg once weekly. Antibiotic-associated colitis, other su-
Maximum: 1,200 mg/dose or 5 mg/kg perinfections may result from altered
once daily. Maximum: 250 mg/dose. bacterial balance in GI tract. Acute in-
terstitial nephritis, hepatotoxicity occur
MAC Treatment rarely.
PO: ADULTS, ELDERLY: 500–600 mg/
day with ethambutol. CHILDREN: 10–12 NURSING CONSIDERATIONS
mg/kg/day (maximum: 500 mg) with
BASELINE ASSESSMENT
ethambutol.
Question for history of hepatitis, allergies
Otitis Media to azithromycin, erythromycins. Assess
PO: CHILDREN 6 MOS AND OLDER: 30 for infection (WBC count, appearance of
mg/kg as single dose (maxi- wound, evidence of fever).
mum: 1,500 mg) or 10 mg/kg/day
INTERVENTION/EVALUATION
for 3 days (maximum: 500 mg) or
10 mg/kg on day 1 (maximum: 500 Check for GI discomfort, nausea, vomit-
mg), then 5 mg/kg on days 2–5 (maxi- ing. Monitor daily pattern of bowel activity
mum: 250 mg). and stool consistency. Monitor LFT, CBC.
Assess for hepatotoxicity: malaise, fever,
Pharyngitis, Tonsillitis abdominal pain, GI disturbances. Be alert
12 mg/
PO: ADULTS, ELDERLY, CHILDREN: for superinfection: fever, vomiting, diar-
kg (maximum: 500 mg) on day 1, then rhea, anal/genital pruritus, oral mucosal
6 mg/kg (maximum: 250 mg) on days changes (ulceration, pain, erythema).
2–5.
PATIENT/FAMILY TEACHING
Pneumonia, Community-Acquired • Continue therapy for full length of
PO: (Zmax): ADULTS, ELDERLY: 2 g as treatment. • Avoid concurrent ad-
single dose. ministration of aluminum- or magne-
PO: ADULTS, ELDERLY, CHILDREN 16 YRS sium-containing antacids. • Bacterial
AND OLDER: 500 mg on day 1, then conjunctivitis: Do not wear contact
250 mg on days 2–5 or 500 mg/day lenses.
IV for 2 days, then 500 mg/day PO to
underlined – top prescribed drug
aztreonam 107
A
in pts younger than 9 mos. Elderly: Age-
aztreonam related renal impairment may require
dosage adjustment.
az-tree-o-nam
(Azactam, Cayston) INTERACTIONS
uCLASSIFICATION DRUG: None significant. HERBAL: None
significant. FOOD: None known. LAB
PHARMACOTHERAPEUTIC: Mono- VALUES: May increase serum alkaline
bactam. CLINICAL: Antibiotic. phosphatase, creatinine, LDH, ALT, AST
levels. Produces a positive Coombs’ test.
USES May prolong partial thromboplastin time
(PTT), prothrombin time (PT).
Injection: Treatment of infections
caused by susceptible gram-negative AVAILABILITY (Rx)
microorganisms P. aeruginosa, E. coli,
Injection, Infusion Solution: (Azac-
S. marcescens, K. pneumoniae, P. mirabi­­­
tam): Premix 1 g/50 mL, 2 g/50 mL. In-
lis, H. influenzae, Enterobacter, Citro­
jection, P
­ owder for Reconstitution: (Azac-
bacter spp., including lower respiratory
tam): 1 g, 2 g. Oral Inhalation, Powder for
tract, skin/skin structure, intraabdominal,
Reconstitution: (Cayston): 75 mg.
gynecologic, complicated/uncomplicated
UTIs; septicemia; cystic fibrosis. Oral in- ADMINISTRATION/HANDLING
halation: (Cayston): Improve respiratory
symptoms in cystic fibrosis pts with P. ae­ IV
ruginosa. OFF-LABEL: Surgical prophylaxis. Reconstitution • For IV push, dilute
each gram with 6–10 mL Sterile Water
PRECAUTIONS for Injection. • For intermittent IV infu-
Contraindications: Hypersensitivity to sion, further dilute with 50–100 mL D5W
aztreonam. Cautions: History of allergy, or 0.9% NaCl. Final concentration not to
esp. cephalosporins, penicillins; renal exceed 20 mg/mL.
impairment; bone marrow transplant Rate of administration • For IV
pts with risk factors for toxic epidermal push, give over 3–5 min. • For IV infu-
necrolysis (TEN). sion, administer over 20–60 min.
Storage • Store vials at room tempera-
ACTION ture. • Solution appears colorless to light
Binds to penicillin-binding proteins, yellow. • Following reconstitution, solu-
which inhibits bacterial cell wall synthe- tion is stable for 48 hrs at room ­temperature
sis. Therapeutic Effect: Bactericidal. or 7 days if refrigerated. • Discard if pre-
cipitate forms. Discard unused portions.
PHARMACOKINETICS
IM
Completely absorbed after IM adminis- • Reconstitute with at least 3 mL diluent
tration. Protein binding: 56%–60%. Par- per gram of aztreonam. • Shake im-
tially metabolized by hydrolysis. Primarily mediately, vigorously after adding dilu-
excreted unchanged in urine. Removed ent. • Inject deeply into large muscle
by hemodialysis. Half-life: 1.4–2.2 hrs mass. • Following reconstitution, solu-
(increased in renal/hepatic impairment). tion is stable for 48 hrs at room tempera-
LIFESPAN CONSIDERATIONS ture or 7 days if refrigerated.
Pregnancy/Lactation: Crosses pla- Inhalation
centa, distributed in amniotic fluid; • Administer only with an Altera nebu-
low concentration in breast milk. Chil- lizer system. • Nebulize over 2–3
dren: Safety and efficacy not established min. • Give bronchodilator 15 min–4
Canadian trade name Non-Crushable Drug High Alert drug
108 aztreonam
A
hrs (short-acting) or 30 min–12 hrs Creatinine
(long-acting) before administra- Clearance Dosage
tion. • Reconstituted solution must be 10–30 mL/min 50% usual dose at
used immediately. usual intervals
Less than 10 mL/ 25% usual dose at
IV INCOMPATIBILITIES min usual intervals
Hemodialysis 500 mg–2 g, then
Acyclovir (Zovirax), amphotericin (Fungi- 25% of initial dose
zone), LORazepam (Ativan), metroNIDA- at usual interval
ZOLE (Flagyl), vancomycin (Vancocin). Continuous renal 2 g, then 1 g q8–12h
replacement or 2g q12h
IV COMPATIBILITIES therapy (CRRT)
Bumetanide (Bumex), calcium gluco-
nate, cimetidine (Tagamet), diltiaZEM Dosage in Hepatic Impairment
(Cardizem), diphenhydrAMINE (Bena- Use with caution.
dryl), DOBUTamine (Dobutrex), DOPa- SIDE EFFECTS
mine (Intropin), famotidine (Pepcid),
furosemide (Lasix), heparin, HYDRO- Frequent (greater than 5%): Cayston:
morphone (Dilaudid), insulin (regular), Cough, nasal congestion, wheezing,
magnesium sulfate, morphine, potassium ­pharyngolaryngeal pain, pyrexia, chest dis-
chloride, propofol (Diprivan). comfort, abdominal pain, vomiting. Occa-
sional (less than 3%): Discomfort and swell-
INDICATIONS/ROUTES/DOSAGE ing at IM injection site, nausea, vomiting,
Severe Infections
diarrhea, rash. Rare (less than 1%): Phlebi-
2 g q6–8h. Maxi-
IV: ADULTS, ELDERLY:
tis or thrombophlebitis at IV injection site,
mum: 8 g/day. CHILDREN: 30 mg/kg abdominal cramps, headache, hypotension.
q6–8h. Maximum: 8 g/day (120 mg/ ADVERSE EFFECTS/TOXIC
kg/day). REACTIONS
Mild to Moderate Infections Antibiotic-associated colitis, other su-
IV: ADULTS, ELDERLY: 1–2 g q8–12h. Max- perinfections may result from altered
imum: 8 g/day. CHILDREN: 30 mg/kg q8h. bacterial balance in GI tract. Severe
Maximum: 8 g/day (120 mg/kg/day). hypersensitivity reactions, including
­
anaphylaxis, occur rarely.
UTI
IM/IV: ADULTS, ELDERLY: 0.5–1 g q8–12h. NURSING CONSIDERATIONS
Usual Neonatal Dosage BASELINE ASSESSMENT
IV: 30 mg/kg/dose q6–12h. Question for history of allergies, esp. to
aztreonam, other antibiotics.
Cystic Fibrosis
Note: Pretreatment with a bronchodila- INTERVENTION/EVALUATION
tor is recommended. Evaluate for phlebitis, pain at IM injection
IV: CHILDREN: 50 mg/kg/dose q6–8h up to site. Assess for GI discomfort, nausea, vom-
200 mg/kg/day. Maximum: 8 g/day. Inha- iting. Monitor daily pattern of bowel activ-
lation (nebulizer): ADULTS, CHILDREN 7 YRS ity, stool consistency. Assess skin for rash.
OR OLDER: 75 mg 3 times/day (at least 4 hrs Be alert for superinfection: fever, vomiting,
apart) for 28 days, then off for 28-day cycle. diarrhea, anal/genital pruritus, oral muco-
Dosage in Renal Impairment sal changes (ulceration, pain, erythema).
Dosage and frequency are modified Monitor renal/hepatic function.
based on creatinine clearance and sever- PATIENT/FAMILY TEACHING
ity of infection: • Report nausea, vomiting, diarrhea, rash.

underlined – top prescribed drug


baclofen 109
PHARMACOKINETICS
baclofen Well absorbed from GI tract. Protein B
binding: 30%. Partially metabolized in
bak-loe-fen liver. Primarily excreted in urine. Half-
(Gablofen, Lioresal) life: 2.5–4 hrs.
j BLACK BOX ALERT jAbrupt
withdrawal of intrathecal form has LIFESPAN CONSIDERATIONS
resulted in severe hyperpyrexia, ob-
tundation, rebound or exaggerated Pregnancy/Lactation: Unknown if
spasticity, muscle rigidity, leading crosses placenta or distributed in breast
to organ failure, death. milk. Children: Safety and efficacy not
Do not confuse baclofen with established in pts younger than 12 yrs.
Bactroban or Beclovent, or Limited published data in children. El-
Lioresal with lisinopril or derly: Increased risk of CNS toxicity
Lotensin. (hallucinations, sedation, confusion, men-
tal depression); age-related renal impair-
uCLASSIFICATION ment may require decreased dosage.
PHARMACOTHERAPEUTIC: Skeletal
muscle relaxant. CLINICAL: Antispas- INTERACTIONS
tic, analgesic in trigeminal neuralgia. DRUG: CNS depressants (e.g., alco-
hol, morphine, oxyCODONE, zol-
pidem) may increase CNS depressant
USES effect. HERBAL: Herbals with sedative
Oral: Management of reversible spastic- properties (e.g., chamomile, kava
ity associated with multiple sclerosis, kava, valerian) may increase CNS
spinal cord lesions. Intrathecal: Man- depression. FOOD: None known. LAB
agement of severe spasticity of spinal VALUES: May increase serum ALT, AST,
cord or cerebral origin in pts 4 yrs of age alkaline phosphatase, glucose.
and older. OFF-LABEL: Treatment of blad-
der spasms, spasticity in cerebral palsy, AVAILABILITY (Rx)
intractable hiccups or pain, Huntington’s 50 mcg/
Intrathecal Injection Solution:
chorea, trigeminal neuralgia. mL, 500 mcg/mL, 1,000 mcg/mL, 2,000
mcg/mL. Tablets: 10 mg, 20 mg.
PRECAUTIONS
Contraindications: Hypersensitivity to ba- ADMINISTRATION/HANDLING
clofen. Intrathecal: IV, IM, SQ, or epi- PO
dural administration in addition to intra- • Give with food or milk. • Tablets
thecal use. Cautions: Renal impairment, may be crushed.
seizure disorder, elderly, autonomic dys-
reflexia, reduced GI motility, GI or uri- Intrathecal
nary obstruction; respiratory, pulmonary, • For screening, a 50 mcg/mL concen-
peptic ulcer disease. tration should be used for injec-
tion. • For maintenance therapy, solu-
ACTION tion should be diluted for pts who
Inhibits transmission of monosynaptic or require concentrations other than 500
polysynaptic reflexes at spinal cord level mcg/mL or 2,000 mcg/mL.
possibly by hyperpolarization of primary
afferent fiber terminals. Therapeutic INDICATIONS/ROUTES/DOSAGE
Effect: Relieves muscle spasticity. b ALERT c Avoid abrupt withdrawal.

Canadian trade name Non-Crushable Drug High Alert drug


110 baricitinib
Spasticity
NURSING CONSIDERATIONS
B PO: ADULTS, CHILDREN 12 YRS AND
OLDER: Initially, 5 mg 3 times daily. May BASELINE ASSESSMENT
increase by 15 mg/day (5 mg/dose) at Record onset, type, location, duration of
3-day intervals until optimal response muscular spasm, pain. Check for immo-
achieved. Range: 40–80 mg/day. Maxi- bility, stiffness, swelling.
mum: 80 mg/day. ELDERLY: Initially,
5 mg 2–3 times daily. May gradually in- INTERVENTION/EVALUATION
crease dosage. For pts on long-term therapy, BMP, LFT,
CBC should be performed periodically.
Intrathecal Dose Assess for paradoxical reaction. Observe
ADULTS, ELDERLY, CHILDREN 4 YRS AND for drowsiness, dizziness, ataxia. Assist
OLDER: Initially, 50 mcg as screening dose with ambulation at all times. Evaluate for
(25 mcg in very small pediatric pts) for 1 therapeutic response: decreased intensity
dose; observe pt for 4–8 hrs for positive of skeletal muscle spasm, pain.
response (decrease in muscle tone and/
or frequency and/or severity of spasm). If PATIENT/FAMILY TEACHING
response is inadequate, give 75 mcg 24h • Drowsiness usually diminishes with
after 1st dose. If response is still inad- continued therapy. • Avoid tasks that
equate, give 100 mcg 24h after 2nd dose. require alertness, motor skills until re-
Initial pump dose: give double screening sponse to drug is established. • Do not
dose (unless efficacy of bolus maintained abruptly withdraw medication after long-
greater than 8 hrs, then screening dose). term therapy (may result in muscle rigid-
After 24h, dose may be increased/de- ity, rebound spasticity, high fever, altered
creased only once q24h until satisfactory mental status). • Avoid alcohol, CNS
response. depressants.
Dosage in Renal Impairment
Use caution.
Dosage in Hepatic Impairment
baricitinib
No dose adjustment. bar-i-sye-ti-nib
SIDE EFFECTS (Olumiant)
Frequent (greater than 10%): Transient j BLACK BOX ALERT jIncreased
risk for developing bacterial, viral,
drowsiness, asthenia, dizziness, nausea, invasive fungal infections including
vomiting. Occasional (10%–2%): Head- tuberculosis, cryptococcosis,
ache, paresthesia, constipation, an- pneumocystosis, that may lead to
orexia, hypotension, confusion, nasal hospitalization or death. Infections
often occurred in combination with
congestion. Rare (less than 1%): Para- immunosuppressants (methotrex-
doxical CNS excitement or restlessness, ate, other disease-modifying
slurred speech, tremor, dry mouth, diar- antirheumatic drugs). Closely moni-
rhea, nocturia, impotence. tor for development of infection.
Test for latent tuberculosis prior
ADVERSE EFFECTS/TOXIC to treatment and during treatment,
REACTIONS regardless of initial result. Treat-
ment of latent TB should be initi-
Abrupt discontinuation may produce hal- ated before initiation. Lymphomas,
lucinations, seizures. Overdose results in other malignancies were reported.
blurred vision, seizures, myosis, mydria- Thromboembolic events including
DVT, pulmonary embolism, arterial
sis, severe muscle weakness, strabismus, thrombosis have occurred.
respiratory depression, vomiting.

underlined – top prescribed drug


baricitinib 111

Do not confuse baricitinib with ACTION


ceritinib, gefitinib, pacritinib, Inhibits JAK enzymes, which are intra- B
tofacitinib, or sunitinib. cellular enzymes involved in stimulating
hematopoiesis and immune cell function
uCLASSIFICATION via a signaling pathway. Therapeutic Ef-
PHARMACOTHERAPEUTIC: Janus- fect: Reduces inflammation, tenderness,
associated kinase inhibitor. CLINI- swelling of joints; slows or prevents pro-
CAL: Antirheumatic agent. Disease gressive joint destruction in rheumatoid
modifying. arthritis (RA).
PHARMACOKINETICS
USES Rapidly absorbed and widely distributed.
Treatment of adults with moderately to Metabolized in liver. Protein binding:
severely active rheumatoid arthritis who 50%. Peak plasma concentration: 1 hr.
have had an inadequate response to one Excreted in urine (75%), feces (20%).
or more TNF antagonist therapies. May be Half-life: 12 hrs.
used alone or in combination with meth-
otrexate or other nonbiologic disease- LIFESPAN CONSIDERATIONS
modifying antirheumatic drugs DMARDs. Pregnancy/Lactation: Unknown if dis­
tributed in breast milk. Breastfeeding not
PRECAUTIONS recommended. Children: Safety and
Hypersensitivity to baricitinib. Cau- efficacy not established. Elderly: In-
tions: Baseline anemia, lymphopenia, creased risk for serious infections, ma-
neutropenia; hepatic/renal impairment, lignancy.
elderly, hypercholesterolemia; history
of arterial or venous thromboembolic INTERACTIONS
events (CVA, DVT, MI, PE), pts at risk DRUG: May diminish therapeutic effects
for thrombosis (immobility, indwelling of live vaccines, BCG (intravesical).
venous catheter/access device, mor- Immunosuppressants (e.g., azathio-
bid obesity, underlying atherosclerosis, prine, cyclosporine) may increase risk
genetic hypercoagulable conditions); for added immunosuppression, infec-
recent travel or residence in TB or my- tion. May enhance adverse/toxic effects
cosis endemic areas; history of chronic of biologic disease-modifying drugs
opportunistic infections (esp. bacterial, (DMARDs), natalizumab, tacroli-
invasive fungal, mycobacterial, protozoal, mus, tofacitinib, vaccines (live).
viral, TB); history of HIV, herpes zoster, Probenecid may increase concentra-
hepatitis B or C virus infection; condi- tion of baricitinib. HERBAL: St. John’s
tions predisposing to infection (e.g., wort may decrease concentration/effect.
diabetes, renal failure, immunocompro- FOOD: None known. LAB VALUES: May
mised pts, open wounds), pts at risk for increase serum ALT, AST, CPK, cholesterol
GI perforation (e.g., Crohn’s disease, di- (HDL, LDL, total), triglycerides; platelets.
verticulitis, GI tract malignancies, peptic May decrease ANC, Hgb, absolute lym-
ulcers, peritoneal malignancies), pts who phocyte count.
reside or travel to where TB is endemic.
Concomitant use of strong organic anion AVAILABILITY (Rx)
transporter 2 (OAT3) inhibitors (e.g., Tablets: 2 mg.
probenecid), JAK inhibitors, biologic
DMARDs, potent immunosuppressants ADMINISTRATION/HANDLING
(e.g., azathioprine or cyclosporine) not PO
recommended. • Give without regard to food.

Canadian trade name Non-Crushable Drug High Alert drug


112 baricitinib

INDICATIONS/ROUTES/DOSAGE other opportunistic infection) may oc-


B b ALERT c Do not initiate in pts with cur. Serious infections may include
severe, active infection (systemic/local- aspergillosis, BK virus, cellulitis, crypto-
ized), absolute lymphocyte count less coccosis, cytomegalovirus, esophageal
than 500 cells/mm3, ANC less than 1000 candidiasis, herpes zoster histoplasmo-
cells/mm3, Hgb less than 8 g/dL. Do not sis, listeriosis, pneumocystosis, pneu-
use in combination with biologic monia, tuberculosis, UTI, sepsis. Upper
DMARDs or with strong immunosuppres- respiratory tract infections including
sants (e.g., azathioprine or cyclospo- epiglottitis, laryngitis, nasopharyngi-
rine). tis, pharyngitis, pharyngotonsillitis,
sinusitis, tracheitis, tonsillitis reported
Rheumatoid Arthritis
in 16% of pts. May increase risk new
PO: ADULTS, ELDERLY: 2 mg once daily.
malignancies. May induce viral reac-
Dose Modification tivation of hepatitis B or C virus infec-
Anemia tion, herpes zoster, HIV. Thrombosis
Hgb less than 8 g/dL: Withhold treat- including DVT, pulmonary embolism,
ment until Hgb is greater than or equal arterial thrombosis have occurred. May
to 8 gm/dL. increase risk of GI perforation. Platelet
Lymphopenia count greater than 600,000 cells/mm3
Absolute lymphocyte count (ALC) occurred in 1% of pts.
less than 500 cells/mm3: Withhold
NURSING CONSIDERATIONS
treatment until ALC is greater than or
equal to 500 cells/mm3. BASELINE ASSESSMENT
Neutropenia
Obtain CBC, BMP, LFT, lipid panel;
ANC less than 1000 cells/mm3: With-
pregnancy test in females of reproduc-
hold treatment until ANC is greater than
3 tive potential. Assess onset, location,
or equal to 1000 cells/mm .
duration of pain, inflammation. In-
Serious Infection
spect appearance of affected joints for
Withhold treatment until serious infec-
immobility, deformities. Evaluate for
tion is resolved, then resume as clinically
active TB and test for latent infection
indicated.
prior to and during treatment. Indura-
Dosage in Renal Impairment tion of 5 mm or greater with purified
eGFR less than 60 mL/min: Not rec- protein derivative (PPD) is consid-
ommended. ered a positive result when assessing
for latent TB. Consider treatment with
Dosage in Hepatic Impairment antimycobacterial therapy in pts with
Mild to moderate impairment: No latent TB. Question history of arte-
dose adjustment. Severe impairment: rial/venous thrombosis, hepatic/renal
Not recommended. impairment, HIV infection, hepatitis B
or C virus infection, diverticulitis, ma-
SIDE EFFECTS lignancies. Screen for active infection.
Rare (2%–1%): Nausea, acne. Assess skin for open wounds. Receive
full medication history and screen for
ADVERSE EFFECTS/TOXIC interactions.
REACTIONS
INTERVENTION/EVALUATION
Neutropenia, lymphopenia may in-
crease risk of infection. Serious and Assess for therapeutic response: relief
sometimes fatal infections (bacterial, of pain, stiffness, swelling; increased
mycobacterial, viral, invasive fungal, joint mobility; reduced joint tender-
ness; improved grip strength. Monitor

underlined – top prescribed drug


basiliximab 113
CBC, LFT periodically. Monitor for TB
regardless of baseline PPD. Consider basiliximab B
discontinuation if acute infection,
opportunistic infection, sepsis oc- ba-si-lik-si-mab
curs; initiate appropriate antimicro- (Simulect)
bial therapy. Immediately report any j BLACK BOX ALERT jMust
hemorrhaging, melena, abdominal be prescribed by a physician
experienced in immunosuppres-
pain, hemoptysis (may indicate GI sion therapy and organ transplant
perforation). Monitor for symptoms management.
of DVT (leg or arm pain/swelling), Do not confuse basiliximab with
CVA (aphasia, altered mental status, daclizumab or brentuximab.
headache, hemiplegia, vision loss),
MI (chest pain, dyspnea, syncope, uCLASSIFICATION
diaphoresis, arm/jaw pain), PE (chest PHARMACOTHERAPEUTIC: Mono-
pain, dyspnea, tachycardia). clonal antibody. CLINICAL: Immuno-
suppressive.
PATIENT/FAMILY TEACHING
• Treatment may depress your immune
system response and reduce your ability USES
to fight infection. Report symptoms of Adjunct with cycloSPORINE, corticoste-
infection such as body aches, chills, roids in prevention of acute organ re-
cough, fatigue, fever. Avoid those with jection in pts receiving renal transplant.
active infection. • Expect routine tu- OFF-LABEL: Treatment of refractory graft-
berculosis screening. Report any travel vs-host disease, prevention of liver or
plans to possible endemic areas. • Do cardiac transplant rejection.
not receive live vaccines. • Report
symptoms of DVT (swelling, pain, hot PRECAUTIONS
feeling in the arms or legs; discolor- Contraindications: Hypersensitivity to basil-
ation of extremity), lung embolism (dif- iximab. Cautions: Re-exposure to sub-
ficulty breathing, chest pain, rapid sequent courses of basiliximab.
heart rate), stroke (confusion, one-
sided weakness or paralysis, difficulty ACTION
speaking). • Treatment may cause Binds to and blocks receptor of inter-
life-threatening arterial blood clots; re- leukin-2, a protein that stimulates pro-
port symptoms of heart attack (chest liferation of T-lymphocytes, which play a
pain, difficulty breathing, jaw pain, nau- major role in organ transplant rejection.
sea, pain that radiates to the arm or jaw, Therapeutic Effect: Impairs response
sweating), stroke (blindness, confusion, of immune system to antigens, prevents
one-sided weakness, loss of conscious- acute renal transplant rejection.
ness, trouble speaking, seizures). • Re-
port symptoms of liver problems such PHARMACOKINETICS
as bruising, confusion, dark or amber- Half-life: 4–10 days (adults); 5–17 days
colored urine, right upper abdominal (children).
pain, or yellowing of the skin or
eyes. • Immediately report severe or LIFESPAN CONSIDERATIONS
persistent abdominal pain, bloody Pregnancy/Lactation: Unknown if
stool, fever; may indicate tear in GI cros­ses placenta or distributed in breast
tract. • Treatment may cause reactiva- milk. Breastfeeding not recommended.
tion of chronic viral infections, new Children/Elderly: No age-related pre-
cancers. cautions noted.

Canadian trade name Non-Crushable Drug High Alert drug


114 basiliximab

INTERACTIONS Dosage in Renal/Hepatic Impairment


B DRUG: May decrease therapeutic effect No dose adjustment.
of BCG (intravesical), vaccines (live). SIDE EFFECTS
May increase adverse effects of belim-
umab, natalizumab, vaccines (live). Frequent (greater than 10%): GI distur-
HERBAL: Echinacea may decrease thera-
bances (constipation, diarrhea, dyspep-
peutic effect. FOOD: None known. LAB sia), CNS effects (dizziness, headache,
VALUES: May alter serum calcium, glu-
insomnia, tremor), respiratory tract in-
cose, potassium; Hgb, Hct. May increase fection, dysuria, acne, leg or back pain,
serum cholesterol, BUN, creatinine, uric peripheral edema, hypertension. Occa-
sional (10%–3%): Angina, neuropathy,
acid. May decrease serum magnesium,
phosphate; platelet count. abdominal distention, tachycardia, rash,
hypotension, urinary disturbances (uri-
AVAILABILITY (Rx) nary frequency, genital edema, hematu-
Injection, Powder for Reconstitution: 10 mg, ria), arthralgia, hirsutism, myalgia.
20 mg. ADVERSE EFFECTS/TOXIC
ADMINISTRATION/HANDLING REACTIONS
Severe, acute hypersensitivity reactions
IV including anaphylaxis characterized by
Reconstitution • Reconstitute 10-mg bronchospasm, capillary leak syndrome,
vial with 2.5 mL or 20-mg vial with 5 mL cytokine release syndrome, dyspnea, HF,
Sterile Water for Injection. • Shake hypotension, pulmonary edema, pruritus,
gently to dissolve. • May further dilute respiratory failure, tachycardia, rash, urti-
with 25–50 mL 0.9% NaCl or D5W to a caria, wheezing have been reported. May
final concentration of 0.4 mg/ increase risk of cytomegalovirus infection.
mL. • Gently invert to avoid foam-
ing. • Do not shake. NURSING CONSIDERATIONS
Rate of administration • Give as IV BASELINE ASSESSMENT
bolus over 10 min or as IV infusion over
Obtain baseline CBC, BMP, serum ionized
20–30 min.
calcium, phosphate, uric acid; vital signs,
Storage • Refrigerate unused vi-
particularly B/P, pulse rate. Question cur-
als. • After reconstitution, use within 4
rent breastfeeding status.
hrs (24 hrs if refrigerated). • Discard
if precipitate forms. INTERVENTION/EVALUATION
Diligently monitor CBC, electrolytes, re-
IV INCOMPATIBILITIES nal function. Assess B/P for hypertension/
Specific information not available. Do not hypotension, pulse for evidence of tachy-
add other medications simultaneously cardia. Question for GI disturbances,
through same IV line. CNS effects, urinary changes. Monitor for
presence of wound infection, signs of in-
INDICATIONS/ROUTES/DOSAGE fection (fever, sore throat, unusual bleed-
Prophylaxis of Organ Rejection ing/bruising), hypersensitivity reaction.
IV: ADULTS, ELDERLY, CHILDREN WEIGH-
ING 35 KG OR MORE: 20 mg within 2 hrs PATIENT/FAMILY TEACHING
before transplant surgery and 20 mg 4 • Report difficulty in breathing or swallow-
days after transplant. CHILDREN WEIGHING ing, palpitations, bruising/bleeding, rash,
LESS THAN 35 KG: 10 mg within 2 hrs be- itching, swelling of lower extremities, weak-
fore transplant surgery and 10 mg 4 days ness. • Female pts should take measures
after transplant. to avoid pregnancy; avoid breastfeeding.

underlined – top prescribed drug


beclomethasone 115
Decreases response to seasonal, peren-
beclomethasone nial rhinitis. B
be-kloe-meth-a-sone PHARMACOKINETICS
(Beconase AQ, QNASL, QVAR Rapidly absorbed from pulmonary, nasal,
RediHaler) GI tissue. Metabolized in liver. Protein
Do not confuse beclomethasone binding: 87%. Excreted in feces (60%),
with betamethasone or dexa- urine (12%). Half-life: 2–4.5 hrs.
methasone, or Beconase with
baclofen. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if
uCLASSIFICATION
cros­ses placenta or distributed in breast
PHARMACOTHERAPEUTIC: Adreno- milk. Children: Prolonged treatment/
corticosteroid. CLINICAL: Anti-inflam- high do­ sages may decrease short-term
matory, immunosuppressant. growth rate, cortisol secretion. El-
derly: No age-related precautions noted.
USES INTERACTIONS
Inhalation: Maintenance and prophy- DRUG: May enhance hyponatremic
lactic treatment of asthma in pts 5 yrs and effect of desmopressin. May de-
older. Intranasal: Beconase AQ: Relief crease effect of aldesleukin, BCG
of seasonal/perennial rhinitis; prevention (intravesical). May increase ad-
of nasal polyp recurrence after surgical verse effects of loxapine, natali-
removal; treatment of nonallergic rhini- zumab. HERBAL: Echinacea may
tis. QNASL: Treatment of seasonal and decrease effects. FOOD: None known.
perennial allergic rhinitis in pts 4 yrs and LAB VALUES: None significant.
older. OFF-LABEL: Prevention of seasonal
rhinitis (nasal form). AVAILABILITY (Rx)
Inhalation,Oral: 40 mcg/inhalation,
PRECAUTIONS
80 mcg/inhalation. Nasal Inhalation:
Contraindications: Hypersensitivity to be- (Beconase AQ): 42 mcg/inhalation.
clomethasone. Oral Inhalation: Acute (QNASL): 40 mcg/actuation, 80 mcg/
exacerbation of asthma, status asthmati- actuation.
cus. Cautions: Cardiovascular disease,
cataracts, diabetes, elderly, glaucoma, ADMINISTRATION/HANDLING
hepatic/renal impairment, myasthenia Inhalation
gravis, risk for osteoporosis, peptic ul- • Shake container well. • Instruct pt
cer disease, seizure disorder, thyroid to exhale completely, place mouthpiece
disease, ulcerative colitis; following acute between lips, inhale, hold breath as long
MI. Avoid use in pts with untreated viral, as possible before exhaling. • Allow at
fungal, or bacterial systemic infections. least 1 min between inhalations. • Rinse
mouth after each use (decreases dry
ACTION
mouth, hoarseness, thrush).
Controls or prevents inflammation by
altering rate of protein synthesis; de- Intranasal
presses migration of polymorphonuclear • Instruct pt to clear nasal passages as
leukocytes, fibroblasts; reverses capillary much as possible before use. • Tilt
permeability. Therapeutic Effect: In- pt’s head slightly forward. • Insert
halation: Inhibits bronchoconstriction, spray tip into nostril, pointing toward
produces smooth muscle relaxation, nasal passages, away from nasal sep-
decreases mucus secretion. Intranasal: tum. • Spray into one nostril while pt

Canadian trade name Non-Crushable Drug High Alert drug


116 beclomethasone
holds the other nostril closed, concur- (3%–2%): Localized fungal infection
B rently inhaling through nose to permit (thrush). Intranasal: Nasal-crusting
medication as high into nasal passages epistaxis, sore throat, ulceration of nasal
as possible. mucosa. Rare: Inhalation: Transient
bronchospasm, esophageal candidiasis.
INDICATIONS/ROUTES/DOSAGE Intranasal: Nasal and pharyngeal candi-
Asthma diasis, eye pain.
Oral inhalation: (QVAR): ADULTS, EL-
DERLY, CHILDREN 12 YRS AND OLDER: (Pts ADVERSE EFFECTS/TOXIC
not on inhaled corticosteroids): Initially REACTIONS
40–80 mcg twice daily. (Previously on in- Acute hypersensitivity reaction (urticaria,
haled corticosteroids): Initially, 40–320 angioedema, severe bronchospasm)
mcg twice daily. Maximum: 320 mcg occurs rarely. Change from systemic to
twice daily. CHILDREN 5–11 YRS: Initially, local steroid therapy may unmask pre-
40 mcg twice daily. Maximum: 80 mcg viously suppressed bronchial asthma
twice daily. condition.
Rhinitis, Prevention of Recurrence of NURSING CONSIDERATIONS
Nasal Polyps
BASELINE ASSESSMENT
Nasal inhalation: (Beconase AQ):
ADULTS, ELDERLY, CHILDREN 12 YRS AND Establish baseline history for asthma,
OLDER: 1–2 sprays (42 or 84 mcg) in rhinitis. Question for hypersensitivity to
each nostril twice daily. Maximum: 336 corticosteroids.
mcg/day. CHILDREN 6–11 YRS: 1 spray INTERVENTION/EVALUATION
(42 mcg) each nostril twice daily (total
dose: 168 mcg daily). May increase to 2 Monitor respiratory status. Auscultate
sprays (84 mcg) 2 times/day (total dose lung sounds. Observe for signs of oral
336 mcg daily). Once adequate control candidiasis. In pts receiving broncho-
achieved, decrease to 1 spray (42 mcg) dilators by inhalation concomitantly
in each nostril twice daily (total dose: with inhaled steroid therapy, advise use
168 mcg daily). of bronchodilator several minutes be-
fore corticosteroid aerosol (enhances
Allergic Rhinitis penetration of steroid into bronchial
Nasal inhalation: (QNASL): ADULTS, tree).
ELDERLY, CHILDREN 12 YRS AND OLDER: 80 PATIENT/FAMILY TEACHING
mcg/spray: 2 sprays in each nostril daily.
Maximum: 320 mcg (4 sprays/day). • Do not change dose schedule or stop
CHILDREN, 4–11 YRS OF AGE: 40 mcg/
taking drug; must taper off gradually un-
spray: 1 spray each nostril once daily. der medical supervision. • Inhalation:
Maximum: 80 mcg/day. Maintain diligent oral hygiene. • Rinse
mouth with water immediately after inha-
Dosage in Renal/Hepatic Impairment lation (prevents mouth/throat dryness,
No dose adjustment. fungal infection of mouth). • Report
sore throat or mouth. • Intranasal:
SIDE EFFECTS Report symptoms that do not improve;
Frequent: Inhalation (14%–4%): Throat or if sneezing, nasal irritation oc-
irritation, dry mouth, hoarseness, curs. • Clear nasal passages prior to
cough. Intranasal: Nasal burning, mu- use. • Improvement may take days to
cosal dryness. Occasional: Inhalation several weeks.

underlined – top prescribed drug


belatacept 117

PHARMACOKINETICS
belatacept Half-life: 8–10 days. B
bel-at-a-sept LIFESPAN CONSIDERATIONS
(Nulojix)
Pregnancy/Lactation: Unknown if
j BLACK BOX ALERT jMust be cros­ses placenta or distributed in breast
administered by personnel trained
in administration/handling of immu- milk. Must either discontinue breastfeed-
nosuppression therapy. Increased ing or discontinue drug. Children: Safety
risk of malignancies, infection. and efficacy not established. Elderly: No
Increased risk of post-transplant age-related precautions noted.
lymphoproliferative disorder (PTLD),
mainly in central nervous system. INTERACTIONS
Not recommended for hepatic
transplants due to increased risk of DRUG: May decrease therapeutic effect
graft loss, death. of BCG (intravesical), vaccines (live).
May increase adverse effects of belim-
uCLASSIFICATION umab, natalizumab, vaccines (live).
PHARMACOTHERAPEUTIC: Selective HERBAL: Echinacea may reduce effect.
T-cell costimulation blocker. CLINI- FOOD: None known. LAB VALUES: May in-
CAL: Immunosuppressive agent. crease serum potassium, cholesterol, uric
acid, glucose; urine protein. May decrease
serum calcium, magnesium, phosphate,
USES potassium; Hgb, Hct, WBC.
Prevention of acute organ rejection
in pts receiving kidney transplants (in AVAILABILITY (Rx)
combination with basiliximab induction, Lyophilized Powder for Injection: 250 mg
mycophenolate mofetil, corticosteroids). per vial.
For use in Epstein-Barr virus (EBV) sero-
positive kidney transplant recipients. ADMINISTRATION/HANDLING
b ALERT c Use only silicone-free dis-
PRECAUTIONS posable syringe provided. Using differ-
Contraindications: Hypersensitivity to bela­ ent syringe may produce translucent
tacept. Transplant pts who are Epstein- particles. Administer via dedicated line
Barr virus (EBV) seronegative or un- only.
known sero-status. Cautions: History of
IV
opportunistic infections: bacterial, my-
cobacterial, invasive fungal, viral, proto- Reconstitution • Reconstitute vial with
zoal (e.g., histoplasmosis, aspergillosis, 10.5 mL of suitable diluent (0.9% NaCl,
candidiasis, coccidioidomycosis, listerio- D5W or Sterile Water for Injection) using
sis, HIV, tuberculosis, pneumocystosis). provided syringe, 18- to 20-gauge nee-
Recent open wounds, ulcerations. Not dle. • Direct stream to glass wall
recommended in liver transplants. Avoid (avoids foaming). • Swirl gently (do
use of live vaccines. not shake). • Discard if opaque parti-
cles, discoloration, or foreign particles
ACTION are present. • Infusion bag must match
Fusion protein acting as a selective diluent (0.9% NaCl with 0.9% NaCl, D5W
T-cell (lymphocyte) costimulation blocker with D5W; may use Sterile Water for Injec-
(binds to CD80 and CD86 receptors on an- tion with NaCl or D5W). • To mix infu-
tigen presenting cells [APC]). Therapeu- sion bag, withdraw and discard volume
tic Effect: Blocks reaction between APC equal to the volume of reconstituted solu-
and T cells needed to activate T lympho- tion. • Using same silicone-free dispos-
cytes. Prevents renal transplant rejection. able syringe, gently inject reconstituted
Canadian trade name Non-Crushable Drug High Alert drug
118 belatacept
solution into 100- to 250-mL bag (based 5%): Abdominal pain, hypotension, ar-
B on concentration). • Final concentra- thralgia, hematuria, upper respiratory
tion of infusion bag should range from 2 infection, insomnia, nasopharyngitis,
mg/mL to 10 mg/mL. • IV infusion sta- back pain, dyspnea, influenza, dysuria,
ble for 24 hrs at room temperature. bronchitis, stomatitis, anxiety, dizziness,
Rate of administration • Infuse over abdominal pain, muscle tremor, acne,
30 min using infusion set with a 0.2- to alopecia, hyperhidrosis.
1.2-micron low-protein-binding filter.
Storage • Refrigerate vials. • Solu- ADVERSE EFFECTS/TOXIC
tion should be clear to slightly opalescent REACTIONS
and colorless to slightly yellow. • May Serious conditions, including malignan-
refrigerate solution up to 24 hrs. • Dis- cies (esp. skin cancer), progressive mul-
card if reconstituted solution remains at tifocal leukoencephalopathy (caused by
room temperature longer than 24 hrs. JC virus), cytomegalovirus, polyoma virus
nephropathy, viral reactivation (herpes
INDICATIONS/ROUTES/DOSAGE zoster, hepatitis), may occur. Other op-
Note: Dosage based on actual body portunistic infections (bacterial, fungal,
weight at time of transplantation. Do not viral, protozoal) may cause tuberculosis,
modify dose unless a change in body cryptococcal meningitis, Chagas’ disease,
weight is greater than 10%. West Nile encephalitis, Guillain-Barré
syndrome, cerebral aspergillosis. Addi-
Prophylaxis of Acute Kidney Transplant tional complications, including chronic
Rejection (in Combination with an allograft nephropathy, renal tubular ne-
Immunosuppressant) crosis, renal artery necrosis, atrial fibril-
IV: ADULTS, ELDERLY: Initial phase: 10 lation, hematoma at incision site, wound
mg/kg on day 1 (day of transplantation, dehiscence, lymphocele, arteriovenous
prior to implantation), day 5, end of fistula thrombosis, hydronephrosis, uri-
wks 2, 4, 8, and 12 after transplantation. nary incontinence, anti-belatacept anti-
Maintenance: 5 mg/kg end of wk 16 body formation, were reported.
following transplantation, then q4wks
thereafter (plus or minus 3 days). NURSING CONSIDERATIONS
Dosage Modification BASELINE ASSESSMENT
Infusion is based on actual body weight at Obtain baseline CBC, serum chemistries,
the time of transplantation; modify dose renal function, glomerular filtration rate
for weight changes greater than 10% dur- (GFR), serum magnesium, ionized cal-
ing treatment. Prescribed dose must be cium, phosphate, lipid panel, urinalysis.
evenly divisible by 12.5 to match closest Evaluate pt for active tuberculosis or
increment (0, 12.5, 25, 37.5, 50, 62.5, latent infection prior to initiating treat-
75, 87.5, 100) in mg. For example, the ment and periodically during therapy.
actual dose for a 64-kg pt is 637.5 mg or Induration of 5 mm or greater with tu-
650 mg, not 640 mg. berculin skin test should be considered
a positive result when assessing whether
Dosage in Renal/Hepatic Impairment
treatment for latent tuberculosis is nec-
No dose adjustment. essary. Assess baseline mental status
SIDE EFFECTS to compare any worsening cognitive
Frequent (45%–20%): Anemia, diarrhea, symptoms. Obtain Epstein-Barr virus
UTI, peripheral edema, constipation, (EBV) serology prior to treatment (con-
hypertension, pyrexia, nausea, cough, traindicated in pts who are EBV sero-
vomiting, headache. Occasional (19%– negative). Note any skin discoloration,

underlined – top prescribed drug


belimumab 119
ulcers, excoriation, lesions. Question uCLASSIFICATION
history of hypertension/hypotension, PHARMACOTHERAPEUTIC: Mono- B
arrhythmia, diabetes, HIV. Receive full clonal antibody. CLINICAL: Immuno-
medication history. Question possibility suppressant, anti-lupus agent.
of pregnancy.
INTERVENTION/EVALUATION
USES
Monitor B/P, vital signs, I&O, weight. Treatment of adults and children aged
Diligently monitor CBC, renal function, 5 yrs or older with active, autoan-
serum electrolytes (hypokalemia may tibody-positive systemic lupus ery-
result in changes in muscle strength, thematosus (SLE) who are receiving
muscle cramps, altered mental status, standard therapy.
cardiac arrhythmias). Routinely moni-
tor serum glucose levels for new-onset PRECAUTIONS
diabetes after transplantation, corti- Contraindications:Hypersensitivity (ana-
costeroid use. Monitor for fever, ten- phylaxis) to belimumab. Cautions:
derness over transplantation site, skin Severe, active, chronic infections; de-
lesions, changing characteristics of pression, pts at risk for suicide, other
moles, neurologic deterioration related mood changes. Avoid live vaccines within
to PTLD or PML. 30 days before or concurrently with be-
PATIENT/FAMILY TEACHING limumab.
• Therapy may increase risk of malig- ACTION
nancies and life-threatening infections.
• Treatment is given with immunosup- Blocks binding of human B-lymphocyte
pressive therapy with basiliximab induc- stimulator protein to receptors on
tion, corticosteroids. • Report history B-lymphocyte. Therapeutic Effect: Re-
of HIV, opportunistic infections, hepatitis, duces activity of B-cell–mediated immu-
coughing of blood, or close relatives with nity and autoimmune response.
active tuberculosis. • Avoid sunlight, PHARMACOKINETICS
sunlamps. • Seek immediate attention
if toxic reactions occur. • Do not re- Half-life: 19 days.
ceive live vaccines. • Report pregnancy LIFESPAN CONSIDERATIONS
or plans of becoming pregnant. • Ad-
here to strict dosing schedule. • Report Pregnancy/Lactation: Unknown if
chest pain, palpitations, edema, fever, cros­ses placenta or distributed in breast
night sweats, weight loss, swollen glands, milk. Contraception recommended dur-
flu-like symptoms, stomach pain, vomit- ing therapy and for at least 4 wks after
ing, diarrhea, weakness, or urinary discontinuation. Children: Safety and
changes (color, frequency, odor, concen- efficacy not established. Elderly: No
tration, burning, blood). age-related precautions noted.
INTERACTIONS
DRUG: Abatacept, belatacept, etan-
belimumab ercept may increase adverse effects. May
decrease therapeutic effect of BCG (in-
be-lim-oo-mab travesical). May increase adverse effects
(Benlysta) of cyclophosphamide, natalizumab,
Do not confuse belimumab with vaccines (live). HERBAL: Echinacea
bevacizumab. may decrease effect. FOOD: None known.
LAB VALUES: May decrease WBC.

Canadian trade name Non-Crushable Drug High Alert drug


120 belimumab

AVAILABILITY (Rx) Dosage in Renal/Hepatic Impairment


B Lyophilized Powder for Injection: 120
No dose adjustment.
mg, 400 mg. Single-Dose Prefilled Sy- SIDE EFFECTS
ringe: 200 mg/mL.
Frequent (15%–12%): Nausea, diarrhea. Oc-
ADMINISTRATION/HANDLING casional (10%–5%): Pyrexia, nasopharyn-
Reconstitution • Allow vial to warm gitis, bronchitis, insomnia, extremity pain,
to room temperature (10–15 depression, migraine, pharyngitis. Rare
(less than 4%): Cystitis, viral gastroenteritis.
min). • Reconstitute 120-mg vial with
1.5 mL Sterile Water for Injection or 400- ADVERSE EFFECTS/TOXIC
mg vial with 4.8 mL Sterile Water for In- REACTIONS
jection (both vials will equal final con-
centration of 80 mg/mL). • Direct May increase risk of mortality. Anti-belim-
stream toward glass wall to avoid foam- umab antibody formation reported in less
ing. • Gently swirl for 60 sec every 5 than 1%. Hypersensitivity reaction, includ-
min until fully dissolved (usually 10–30 ing anaphylactic reaction, may include
min). • If mechanical reconstitution urticaria, pruritus, erythema, dyspnea, an-
device is used, do not swirl greater than gioedema, hypotension (13% of pts). Infu-
30 min or exceed 500 rpm. • Small air sion reactions such as nausea, headaches,
bubbles expected, acceptable. • Dilute flushing occur more frequently. Serious
in 250 mL 0.9% NaCl only. • From infu- infections related to immunosuppres-
sion bag, withdraw and discard volume sion, including respiratory tract infection,
equal to the volume of reconstituted so- pneumonia, nasopharyngitis, sinusitis,
lution. • Invert bag and gently inject influenza, UTI, cellulitis, bronchitis, viral
solution to mix. • Infuse within 8 hrs of reactivation, may occur. Mental health is-
reconstitution. sues, including psychiatric events (16%)
and depression (6%), have been noted.
Rate of administration • Infuse over Life-threatening psychiatric events and
1 hr. depression (including suicide) reported
Storage • Refrigerate vials/infusion in less than 1%. Pts who experienced life-
bag until time of use. • Solution should threatening episodes had prior psychiatric
be opalescent and colorless to pale yel- history.
low with no particles present. • Dis-
card solution if particulate matter or NURSING CONSIDERATIONS
discoloration observed. • Protect from BASELINE ASSESSMENT
sunlight.
Obtain baseline CBC with differential,
IV INCOMPATIBILITIES BMP, IgG level, vital signs. Assess history
Do not infuse with dextrose-based solu- of recent immunizations, malignancies,
tion. Use dedicated line only. open sores, ulcerations, weight loss, HIV
infection, chronic infection. Assess psychi-
INDICATIONS/ROUTES/DOSAGE atric history, including insomnia, anxiety,
Active Systemic Lupus Erythematosus
depression, impulsiveness, suicidal ide-
Note: When switching from IV to SQ, ations, mood changes. Question possibility
give first SQ dose 1–4 wks after the last of pregnancy, current breastfeeding.
IV dose. INTERVENTION/EVALUATION
IV: ADULTS, ELDERLY, CHILDREN 5 YRS AND Monitor vital signs, CBC. If hypersensitiv-
OLDER: Initially, 10 mg/kg q2wks for 3 ity reaction occurs, immediately notify
doses, then q4wks thereafter. physician. Premedication with antihista-
SQ: ADULTS, ELDERLY: 200 mg once weekly. mines, antipyretics, and/or corticoste-

underlined – top prescribed drug


belinostat 121
roids may prevent subsequent reactions. bocytopenia. Avoid use in pts with active
Discontinue treatment if a­naphylactic infection. B
reaction occurs; initiate appropriate
­
medical treatment. Routinely inspect ACTION
skin, paying close attention to areas that Inhibits enzymatic activity of histone
are discolored, irregular, or have ill- deacetylases by catalyzing removal
defined borders (may indicate malignan- of acetyl groups from lysine residues
cies). Obtain anti-belimumab antibody of histones and nonhistone proteins.
titer if immunogenicity suspected. Con- Therapeutic Effect: Inhibits tumor cell
sider interrupting therapy if acute infec- growth and metastasis; causes tumor cel-
tion occurs. lular death (apoptosis).
PATIENT/FAMILY TEACHING PHARMACOKINETICS
• Report any signs of allergic reaction (see Limited tissue distribution. Metabolized
Adverse Effects/Toxic Reactions). in liver. Protein binding: 93%–95%. Ex-
• If anaphylactic reaction occurs, pt may creted primarily in urine. Half-life: 1.1
require rapid-sequence intubation. • Al- hrs.
lergic reactions include itching, hives, dizzi-
ness, or difficulty breathing. • Notify phy- LIFESPAN CONSIDERATIONS
sician if pregnant or plan on becoming Pregnancy/Lactation: Has teratogenic
pregnant. • Contraception recommended effects; may cause fetal harm/demise. Not
during treatment and at least 4 mos after recommended in nursing mothers. Un-
discontinuation. • Report suicidal ide- known if distributed in breast milk. Must
ation, mood changes, or worsening depres- either discontinue drug or discontinue
sion. • Do not receive live vaccines 30 breastfeeding. Children: Safety and ef-
days before or during treatment. • Report ficacy not established. Elderly: No age-
any fever, cough, night sweats, flu-like related precautions noted.
symptoms, skin changes, or painful/burn-
ing urination. INTERACTIONS
DRUG: Strong UGT1A1 inhibitors
(e.g., atazanavir) may increase con-
centration/effect. May decrease thera-
belinostat peutic effect of BCG (intravesical).
HERBAL: None known. FOOD: None
beh-lih-noh-stat significant. LAB VALUES: May decrease
(Beleodaq) ANC, Hgb/Hct, lymphocytes, platelets,
uCLASSIFICATION
WBC; serum potassium. May increase
blood lactic dehydrogenase, serum cre-
PHARMACOTHERAPEUTIC: Histone atinine.
deacetylase (HDAC) inhibitor. CLINI-
CAL: Antineoplastic. AVAILABILITY (Rx)
Lyophilized Powder for Injection: 500 mg
USES vial.
Treatment of relapsed or refractory pe- ADMINISTRATION/HANDLING
ripheral T-cell lymphoma (PTCL).
IV
PRECAUTIONS Reconstitution • Maintain standard
Contraindications: Hypersensitivity to be­ chemotherapy preparation and handling
li­nostat. Cautions: Pts with high tumor precautions. • Reconstitute each vial
burden, hx of hepatic impairment, throm- with 9 mL of Sterile Water for Injection,

Canadian trade name Non-Crushable Drug High Alert drug


122 belinostat
using suitable syringe for final concentration two dosage reductions: Discontinue
B of 50 mg/mL. • Gently swirl contents treatment. Nausea, vomiting, diar-
until completely dissolved. • Visually rhea: Only modify dose if duration is
inspect for particulate matter. • Do not greater than 7 days with supportive man-
use if cloudiness or particulate matter agement. Pts with reduced UGT1A1
observed. • Withdraw required dosage activity: Reduce starting dose to 750
and mix into infusion bag containing 250 mg/m2 in pts known to be homozygous
mL of 0.9% NaCl. for UGT1A1*28 allele.
Rate of administration • Infuse over
30 min using 0.22-micron in-line fil- Dosage in Renal/Hepatic Impairment
ter. • May extend infusion time to 45 No dose adjustment.
min if infusion site pain or other infu-
sion-related symptoms occur. SIDE EFFECTS
Storage • Reconstituted vial may be Frequent (47%–29%): Nausea, fatigue,
stored at room temperature (max 77ºF/ pyrexia, vomiting, anemia. Occasional
25ºC) for up to 12 hrs. • Infusion bag (23%–10%): Constipation, diarrhea, dys-
may be stored at room temperature (max pepsia, rash, peripheral edema, cough,
77ºF/25ºC) for up to 36 hrs. pruritus, chills, decreased appetite,
headache, infusion site pain, abdominal
INDICATIONS/ROUTES/DOSAGE pain, hypotension, phlebitis, dizziness.
Peripheral T-Cell Lymphoma ADVERSE EFFECTS/TOXIC
IV infusion: ADULTS/ELDERLY: 1,000 mg/ REACTIONS
m2 once daily on days 1–5 of a 21-day
cycle. Cycles may be repeated every 21 Anemia, lymphopenia, neutropenia,
days until disease progression or unac- thrombocytopenia are expected responses
ceptable toxicity. to therapy. Serious and sometimes fatal
infections including pneumonia, sepsis
Dose Modification have occurred. May cause hepatotoxicity,
ANC should be greater than or equal to LFT abnormalities, tumor lysis syndrome.
1,000 cells/mm3 and platelet count greater GI toxicities including severe diarrhea,
than or equal to 50,000 cells/mm3 prior to nausea, vomiting may require use of
start of each cycle or prior to resuming antiemetic and antidiarrheal medication
treatment following toxicity. Discontinue or result in dosage reduction. Nineteen
treatment if ANC nadir less than 500 cells/ percent of pts required treatment discon-
mm3 or recurrent platelet count nadir less tinuation related to toxic anemia, febrile
than 25,000 cells/mm3 after two dose re- neutropenia, multiorgan failure, ventric-
ductions. Other toxicities must be Grade 2 ular fibrillation (rare).
or less prior to resuming treatment.
NURSING CONSIDERATIONS
Hematologic Toxicities
BASELINE ASSESSMENT
Platelet count greater than 25,000
cells/mm3 or ANC greater than 500 Obtain baseline ANC, CBC, BMP, LFT, vi-
cells/mm3: No change. Platelet count tal signs; urine pregnancy in women of
less than 25,000 cells/mm3 or ANC reproductive potential. Question history
less than 500 cells/mm3: Decrease of anemia, arrhythmias, hepatic impair-
dose by 25% (750 mg/m2). ment, peripheral edema, or if pt homo-
zygous for UGT1A1 allele (may require
Nonhematologic Toxicities reduced starting dose). Question possi-
Any Grade 3 or 4: Decrease dose by bility of pregnancy, current breastfeeding
25% (750 mg/m2). Recurrence of status. Receive full medication history
Grade 3 or 4 adverse reaction after including herbal products.

underlined – top prescribed drug


benazepril 123

INTERVENTION/EVALUATION USES
Treatment of hypertension. Used alone B
Diligently monitor blood counts (esp. ANC,
Hgb/Hct, WBC, platelet count) weekly; he- or in combination with other antihyper-
patic/renal function prior to start of first tensives.
dose of each cycle, vital signs. Monitor
for symptoms of hypokalemia. Screen for PRECAUTIONS
tumor lysis syndrome (electrolyte imbal- Contraindications: Hypersensitivity to be­
ance, uric acid nephropathy, acute renal nazepril. History of angioedema with
failure). Obtain ECG if arrhythmia, palpita- or without previous treatment with ACE
tions occur. Notify physician if any CTCAE inhibitors. Use with aliskiren in pts
toxicities occur (see Appendix M). Offer with diabetes. Coadministration with or
antiemetics if nausea, vomiting occurs. within 36 hrs of switching to or from
a neprilysin inhibitor (e.g., sacubi-
PATIENT/FAMILY TEACHING tril). Cautions: Renal impairment; hy-
• Blood levels will be routinely moni- pertrophic cardiomyopathy without flow
tored. • Avoid pregnancy; treatment may tract obstruction; severe aortic stenosis;
cause birth defects or miscarriage. Do not before, during, or immediately following
breastfeed. • Report any abdominal pain, major surgery; unstented renal artery
black/tarry stools, bruising, yellowing of stenosis; diabetes mellitus, pregnancy,
skin or eyes, dark urine, decreased urine breastfeeding. Concomitant use of
output. • Severe diarrhea may lead to de- potassium-sparing diuretics, potassium
hydration. • Body aches, burning with supplements.
urination, chills, cough, difficulty breathing,
fever may indicate an acute infection. ACTION
Decreases rate of conversion of angioten-
benazepril sin I to angiotensin II, a potent vasocon-
strictor. Results in lower levels of angio-
tensin II, causing an increase in plasma
ben-ay-ze-pril
renin activity and decreased aldosterone
(Lotensin)
secretion. Therapeutic Effect: Lowers
j BLACK BOX ALERT jMay B/P.
cause fetal injury, mortality. Dis-
continue as soon as possible once
pregnancy is detected. PHARMACOKINETICS
Do not confuse benazepril with Route Onset Peak Duration
enalapril, lisinopril, or Benadryl, PO 1 hr 2–4 hrs 24 hrs
or Lotensin with Lioresal.
Partially absorbed from GI tract. Pro-
FIXED-COMBINATION(S) tein binding: 97%. Metabolized in liver.
Lotensin HCT: benazepril/hydrochlo- Primarily excreted in urine. Minimal
rothiazide (a diuretic): 5 mg/6.25 mg, removal by hemodialysis. Half-life: 35
10 mg/12.5 mg, 20 mg/12.5 mg, 20 min; metabolite, 10–11 hrs.
mg/25 mg. Lotrel: benazepril/amLO-
DIPine (a calcium blocker): 2.5 mg/10 LIFESPAN CONSIDERATIONS
mg, 5 mg/10 mg, 5 mg/20 mg, 5 mg/40 Pregnancy/Lactation: Crosses pla-
mg, 10 mg/20 mg, 10 mg/40 mg. centa. Unknown if distributed in breast
milk. May cause fetal, neonatal mor-
uCLASSIFICATION tality or morbidity. Children: Safety
PHARMACOTHERAPEUTIC: Angio- and efficacy not established. Elderly:
tensin-converting enzyme (ACE) in- May be more sensitive to hypotensive
hibitor. CLINICAL: Antihypertensive. effects.

Canadian trade name Non-Crushable Drug High Alert drug


124 benazepril

INTERACTIONS SIDE EFFECTS


B DRUG: Aliskiren may increase hyperkale- Frequent (6%–3%): Cough, headache, diz-
mic effect. May increase potential for aller- ziness. Occasional (2%): Fatigue, drowsi-
gic reactions to allopurinol. Angioten- ness, nausea. Rare (less than 1%): Rash,
sin II receptor blockers (ARB) (e.g., fever, myalgia, diarrhea, loss of taste.
losartan, valsartan) may increase ad-
verse effects. May increase adverse effects ADVERSE EFFECTS/TOXIC
of lithium, sacubitril. HERBAL: Herb- REACTIONS
als with hypertensive properties (e.g., Excessive hypotension (“first-dose syn-
licorice, yohimbe) or hypotensive cope”) may occur in pts with HF, severe
properties (e.g., garlic, ginger, ginkgo salt or volume depletion. Angioedema,
biloba) may alter effects. FOOD: None hyperkalemia occur rarely. Agranulocy-
known. LAB VALUES: May increase serum tosis, neutropenia may be noted in pts
potassium, ALT, AST, alkaline phosphatase, with renal impairment, collagen vas-
bilirubin, BUN, creatinine, glucose. May de- cular disease (scleroderma, systemic
crease serum sodium; Hgb, Hct. May cause lupus erythematosus). Nephrotic syn-
positive ANA titer. drome may occur in pts with history of
renal disease.
AVAILABILITY (Rx)
Tablets: 5 mg, 10 mg, 20 mg, 40 mg. NURSING CONSIDERATIONS
BASELINE ASSESSMENT
ADMINISTRATION/HANDLING
• Give without regard to food. Obtain CBC before therapy begins and
q2wks for 3 mos, then periodically there-
INDICATIONS/ROUTES/DOSAGE after. Obtain B/P immediately before each
Hypertension (Monotherapy)
dose, in addition to regular monitoring
PO: ADULTS, ELDERLY: Initially, 5–10 (be alert to fluctuations).
mg/day. Titrate based on pt response up to INTERVENTION/EVALUATION
40 mg daily in 1 or 2 divided doses. CHIL- Assist with ambulation if dizziness oc-
DREN 6 YRS AND OLDER: Initially, 0.2 mg/ curs. Monitor B/P, renal function,
kg/day (up to 10 mg/day). Maintenance: urinary protein, serum potassium.
0.1–0.6 mg/kg/day. Maximum: 0.6 mg/ Monitor CBC with differential if pt has
kg or 40 mg/day. collagen vascular disease or renal im-
Hypertension (Combination Therapy)
pairment. If excessive reduction in B/P
PO: ADULTS: Discontinue diuretic 2–3 occurs, place pt in supine position with
days before initiating benazepril, then dose legs elevated. Monitor pt with renal
as noted above. If unable to discontinue impairment, autoimmune disease, or
diuretic, begin benazepril at 5 mg/day. taking drugs that affect leukocytes or
immune response.
Dosage in Renal Impairment PATIENT/FAMILY TEACHING
CrCl less than 30 mL/min: ADULTS: Ini-
tially, 5 mg/day titrated up to maximum of • To reduce hypotensive effect, go from
40 mg/day. CHILDREN: Not recommended. lying to standing slowly. • Full thera-
HD, PD: 25%–50% of usual dose; sup-
peutic effect may take 2–4 wks. • Skip-
plement dose not necessary. ping doses or noncompliance with drug
therapy may produce severe rebound
Dosage in Hepatic Impairment hypertension. • Report dizziness, per-
Use caution. sistent cough.

underlined – top prescribed drug


bendamustine 125

INTERACTIONS
bendamustine DRUG: May decrease therapeutic effect B
of BCG (intravesical). HERBAL: None
ben-da-mus-teen
significant. FOOD: None known. LAB
(Bendeka, Treanda)
VALUES: May increase serum AST, bili-
Do not confuse bendamustine
rubin, creatinine, glucose, uric acid. May
with carmustine or lomustine.
decrease WBCs, neutrophils, Hgb, plate-
uCLASSIFICATION lets; serum potassium, sodium, calcium.
PHARMACOTHERAPEUTIC: Alkylat- AVAILABILITY (Rx)
ing agent. CLINICAL: Antineoplastic.
Injection, Powder for Reconstitution:
(Treanda):  25 mg, 100 mg. Injection:
USES (Bendeka): 100 mg/4 mL.
Treatment of chronic lymphocytic leuke- ADMINISTRATION/HANDLING
mia (CLL). Treatment of indolent B-cell
non-Hodgkin’s lymphoma (NHL) that IV
has progressed during or within 6 mos Reconstitution • Reconstitute each
of treatment with riTUXimab or a riTUX- 100-mg vial with 20 mL Sterile Water for
imab-containing regimen. OFF-LABEL: Injection (25-mg vial with 5 mL) for final
Treatment of mantle cell lymphoma, re- concentration of 5 mg/mL. • Powder
lapsed multiple myeloma. First-line treat- should completely dissolve in 5
ment for follicular lymphoma. Treatment min. • Discard if particulate matter is
of Waldenström’s macroglobulinemia. observed. • Withdraw volume needed
for required dose (based on 5 mg/mL
PRECAUTIONS concentration) and immediately transfer
Contraindications: Hypersensitivity to ben­ to 500-mL infusion bag of 0.9% NaCl for
damustine. (Bendeka only): polyethylene final concentration of 0.2–0.6 mg/
glycol 400, or propylene glycol mono- mL. • Reconstituted solution must be
thioglycerol. Cautions: Myelosuppression transferred to infusion bag within 30 min
(may increase risk of infection), renal/ of reconstitution. • After transferring,
hepatic impairment, dehydration, HF. thoroughly mix contents of infusion bag.
Rate of administration • Infuse over
ACTION 30 min for CLL or 60 min for NHL.
Alkylates and cross-links double-stranded Storage • Reconstituted solution should
DNA. Therapeutic Effect: Inhibits tu- appear clear and colorless to pale yel-
mor cell growth, causes cell death. low. • Final solution is stable for 24
hrs if refrigerated or 3 hrs at room
PHARMACOKINETICS temperature. • Administration must
Metabolized via hydrolysis to metabolites. be completed within these stability time
Protein binding: 64%–95%. Excreted frames.
primarily in feces. Half-life: 40 min.
INDICATIONS/ROUTES/DOSAGE
LIFESPAN CONSIDERATIONS b ALERT c Antiemetics are recom-
Pregnancy/Lactation: May cause fetal mended to prevent nausea and vomiting.
harm. Unknown if distributed in breast
milk. Impaired spermatogenesis, azo- Chronic Lymphocytic Leukemia
ospermia have been reported in male IV infusion: ADULTS/ELDERLY: 100 mg/
pts. Children: Safety and efficacy not m2 given over 30 min daily on days 1 and
established. Elderly: No age-related 2 of a 28-day cycle as a single agent, up
precautions noted. to 6 cycles.

Canadian trade name Non-Crushable Drug High Alert drug


126 benralizumab
Non-Hodgkin’s Lymphoma INTERVENTION/EVALUATION
B IV infusion: ADULTS/ELDERLY: 120 mg/ Offer antiemetics to control nausea,
m2 on days 1 and 2 of a 21-day cycle as a vomiting. Monitor daily pattern of bowel
single agent, up to 8 cycles. activity, stool consistency. Assess skin for
Dose Modification
evidence of rash. Monitor for signs of
Hematologic toxicity Grade 4 or
infection (fever, chills, cough, flu-like
greater: Withhold until ANC 1,000 cells/
symptoms). Monitor for hypertension.
mm3 or greater, platelet 75,000 cells/mm3 Hematologic nadirs occur in 3rd week
or greater. CLL: toxicity Grade 3 or of therapy and may require dose delays if
greater: Reduce dose to 50 mg/m2 on
recovery to recommended values has not
days 1 and 2 of each treatment cycle. Re- occurred by day 28.
currence: Reduce dose to 25 mg/2 on days PATIENT/FAMILY TEACHING
1 and 2 of each cycle. NHL: hematologic • Avoid crowds, those with known infec-
toxicity Grade 4 or nonhematologic tion. • Avoid contact with anyone who
toxicity Grade 3 or greater: Reduce recently received live virus vac-
dose to 90 mg/m2 on days 1 and 2 of each cine. • Do not have immunizations
cycle. Recurrence: Reduce dose to 60 mg/ without physician’s approval (drug low-
m2 on days 1 and 2 of each treatment cycle. ers body resistance). • Promptly report
Dosage in Renal Impairment fever, chills, flu-like symptoms, sore
Not recommended in pts with CrCl less throat, unusual bruising/bleeding from
than 40 mL/min. any site. • Male pts should be warned
of potential risk to their reproductive
Dosage in Hepatic Impairment
capacities.
Mild: Use caution. Moderate to se-
vere: Not recommended.
SIDE EFFECTS
Frequent (24%–16%): Fever, nausea, vom- benralizumab
iting. Occasional (9%–8%): Diarrhea, fa-
tigue, asthenia (loss of strength, energy), ben-ra-liz-ue-mab
rash, decreased weight, nasopharyngitis. (Fasenra)
Rare (6%–3%): Chills, pruritus, cough, Do not confuse benralizumab
herpes simplex infections. with certolizumab, daclizumab,
eculizumab, efalizumab,
ADVERSE EFFECTS/TOXIC mepolizumab, natalizumab,
REACTIONS omalizumab, pembrolizumab,
Myelosuppression characterized as neu- reslizumab, tocilizumab, or
tropenia (75% of pts), thrombocytope- vedolizumab.
nia (77% of pts), anemia (89% of pts),
leukopenia (61% of pts) is an expected uCLASSIFICATION
response to therapy. Infection, including PHARMACOTHERAPEUTIC: Interleu-
pneumonia, sepsis, may occur. Tumor lysis kin-5 receptor alpha-directed cytolytic.
syndrome may lead to acute renal failure. Monoclonal antibody. CLINICAL: An-
Worsening of hypertension occurs rarely. tiasthmatic.
NURSING CONSIDERATIONS
USES
BASELINE ASSESSMENT
Add-on maintenance treatment of pts
Obtain baseline CBC, BMP, LFT before with severe asthma, aged 12 yrs and
treatment begins and routinely thereafter. older, and with an eosinophilic phe-
Question for possibility of pregnancy. Of- notype.
fer emotional support.
underlined – top prescribed drug
benralizumab 127

PRECAUTIONS ­intact. • Visually inspect for particu-


Contraindications: Hypersensitivity to ben­ late matter or discoloration. Solution B
ralizumab. Cautions: History of helminth should appear clear, colorless to slightly
(parasite) infection; long-term use of yellow in color. Do not use if solution is
corticosteroids. Not indicated for treat- cloudy, discolored, or visible particles
ment of other eosinophilic conditions; are observed.
relief of acute bronchospasm or status Administration • Follow manufacturer
asthmaticus. guidelines regarding use of plunger. • In-
sert needle subcutaneously into upper arm,
ACTION outer thigh, or abdomen and inject solu-
Exact mechanism unknown. Inhib- tion. • Do not inject into areas of active
its signaling of interleukin-5 cytokine, skin disease or injury such as sunburns,
reducing production and survival of skin rashes, inflammation, skin infections,
eosinophils responsible for asthmatic or active psoriasis. • Do not administer IV
inflammation and pathogenesis. Thera- or intramuscularly. • Rotate injection
peutic Effect: Prevents inflammatory sites.
process; relieves signs/symptoms of Storage • Refrigerate prefilled sy-
asthma. ringes in original carton until time of use.
Once warmed to room temperature, do
PHARMACOKINETICS not place back into refrigerator. • Do
Widely distributed. Degraded into small not freeze or expose to heating
peptides and amino acids via proteolytic sources. • Do not shake. • Protect
enzymes. Half-life: 15 days. from light.

LIFESPAN CONSIDERATIONS INDICATIONS/ROUTES/DOSAGE


Pregnancy/Lactation: Unknown if Asthma (Severe)
dis­tributed in breast milk. However, hu- SQ: ADULTS, ELDERLY, CHILDREN: 30 mg
man immunoglobulin G is present in once q4wks for the first 3 doses, then
breast milk and is known to cross pla- once q8wks thereafter.
centa. Children: Safety and efficacy not Dosage in Renal/Hepatic Impairment
established in pts younger than 12 yrs. El- Not specified; use caution.
derly: No age-related precautions noted.
SIDE EFFECTS
INTERACTIONS
Occasional (8%–3%): Headache, pyrexia.
DRUG: May increase adverse effects of
belimumab. HERBAL: None significant. ADVERSE EFFECTS/TOXIC
FOOD: None known. LAB VALUES: None REACTIONS
known. Hypersensitivity reactions including ana-
AVAILABILITY (Rx) phylaxis, angioedema, bronchospasm,
hypotension, urticaria, rash were re-
Injection Solution: 30 mg/mL. ported. Hypersensitivity reactions typically
ADMINISTRATION/HANDLING occurred hrs to days after administration.
Infections including bacterial/viral phar-
SQ yngitis may occur. Unknown if treatment
Preparation • Remove prefilled sy- will influence the immunological re-
ringe from refrigerator and allow solu- sponse to helminth (parasite) infection.
tion to warm to room temperature Immunogenicity (auto-benralizumab an-
(approx. 30 min) with needle cap tibodies) reported in 13% of pts.

Canadian trade name Non-Crushable Drug High Alert drug


128 bethanechol

NURSING CONSIDERATIONS uCLASSIFICATION


B PHARMACOTHERAPEUTIC: Parasym-
BASELINE ASSESSMENT pathomimetic choline ester. CLINICAL:
Obtain apical pulse, oxygen saturation. Cholinergic.
Auscultate lung fields. Question history of
parasitic infection, hypersensitivity reaction.
Pts with preexisting helminth (parasite) in- USES
fection should be treated prior to initiation. Treatment of acute postoperative and
Inhaled or systemic corticosteroids should postpartum nonobstructive urinary re-
not be suddenly discontinued upon initia- tention, neurogenic atony of urinary
tion. Corticosteroids that are not gradually bladder with retention. OFF-LABEL: Treat-
reduced may cause withdraw symptoms or ment of gastroesophageal reflux.
unmask conditions that were originally sup-
pressed with corticosteroid therapy. PRECAUTIONS
Contraindications: Hypersensitivity to be­
INTERVENTION/EVALUATION thanechol. Mechanical obstruction of GI/
Monitor rate, depth, rhythm of respirations. GU tract, GI or bladder wall instability,
Assess lungs for wheezing, rales. Monitor hyperthyroidism, asthma, peptic ulcer
oxygen saturation. Interrupt or discontinue disease, epilepsy, pronounced brady-
treatment if hypersensitivity reaction, oppor- cardia or hypotension, parkinsonism,
tunistic infection (esp. parasite infection, her- CAD, vasomotor instability, bladder neck
pes zoster infection); worsening of asthma- obstruction, spastic GI disturbances,
related symptoms (esp. in pts tapering off acute inflammatory lesions of the GI
corticosteroids) occurs. Obtain pulmonary tract, peritonitis, marked vagotonia.
function test to assess disease improvement. Cautions: Bladder reflux infection.
Monitor for increased use of rescue inhalers;
may indicate deterioration of asthma. ACTION
Stimulates parasympathetic nervous
PATIENT/FAMILY TEACHING system, increasing bladder muscle tone
• Treatment not indicated for relief of and causing contractions, which initi-
acute asthmatic episodes. • Have a res- ates urination. Also stimulates gastric
cue inhaler readily available. • In- motility, increasing gastric tone, and
creased use of rescue inhaler may indicate may restore peristalsis. Therapeutic
worsening of asthma. • Seek medical Effect: May initiate urination, bladder
attention if asthma symptoms worsen or emptying. Stimulates gastric, intestinal
remain uncontrolled after starting ther- motility.
apy. • Immediately report allergic reac-
tions such as difficulty breathing, itching, PHARMACOKINETICS
hives, rash, swelling of the face or
Route Onset Peak Duration
tongue. • Report infections of any
kind. • Do not stop corticosteroid ther- PO 30–90 min 60 min 6 hrs
apy unless directed by prescriber. Poorly absorbed following PO adminis-
tration. Does not cross blood-brain bar-
bethanechol rier. Half-life: Unknown.

be-than-e-kole
LIFESPAN CONSIDERATIONS
(Duvoid , Urecholine) Pregnancy/Lactation: Unknown if
Do not confuse bethanechol cros­ses placenta or distributed in breast
with betaxolol. milk. Children/Elderly: No age-related
precautions noted.

underlined – top prescribed drug


bevacizumab 129
OFF-LABEL: Adjunctive therapy in malignant
bevacizumab mesothelioma, ovarian cancer, prostate B
cancer, age-related macular degeneration.
be-va-siz-ue-mab Treatment of metastatic breast cancer.
(Avastin)
j BLACK BOX ALERT jMay result PRECAUTIONS
in development of GI perforation, Contraindications: Hypersensitivity to
presented as intra-abdominal beva­cizumab. Cautions: Cardiovascular
abscess, fistula, wound dehiscence, disease, acquired coagulopathy, preex-
wound healing complications.
Severe, sometimes fatal, hemor- isting hypertension, pts at risk of throm-
rhagic events including central bocytopenia. Pts with CNS metastasis. Do
nervous system/GI/vaginal bleeding, not administer within 28 days of major
epistaxis, hemoptysis, pulmonary surgery or active bleeding.
hemorrhage have occurred.
Do not confuse Avastin with ACTION
Astelin, or bevacizumab with Binds to and neutralizes vascular en-
cetuximab or riTUXimab. dothelial growth factor, preventing as-
uCLASSIFICATION
sociation with endothelial receptors.
Therapeutic Effect: Inhibition of mi-
PHARMACOTHERAPEUTIC: Vascular crovascular growth retards growth of all
endothelial growth factor (VEGF) in- tissue, including metastatic tissue.
hibitor. Monoclonal antibody. CLINI-
CAL: Antineoplastic. PHARMACOKINETICS
Clearance varies by body weight, gen-
USES der, tumor burden. Half-life: 20 days
(range: 11–50 days).
First- or second-line combination che-
motherapy with 5-fluorouracil (5-FU) for LIFESPAN CONSIDERATIONS
treatment of pts with colorectal cancer. Pregnancy/Lactation: May possess tera-
Second-line treatment of colorectal cancer togenic effects. Potential for fertility impair-
after progression of first-line treatment ment. May decrease maternal and fetal body
with bevacizumab. Treatment with CARBO- weight, increase risk of skeletal fetal abnor-
platin and PACLitaxel for nonsquamous, malities. Breastfeeding not recommended.
non–small-cell lung cancer (NSCLC). Children: Safety and efficacy not estab-
Treatment of renal cell carcinoma (meta- lished. Elderly: Higher incidence of severe
static) with interferon alfa, brain can- adverse reactions in pts older than 65 yrs.
cer (glioblastoma) that has progressed
following prior therapy. Treatment of plati- INTERACTIONS
num-resistant recurrent epithelial ovarian, DRUG: May increase cardiotoxic effect
fallopian tube, or primary peritoneal cancer of anthracyclines. May decrease thera-
(in combination with PACLitaxel, DOXOru- peutic effect of BCG (intravesical). May
bicin [liposomal] or topotecan). Treatment increase adverse effects of belimumab.
of stage III or IV epithelial ovarian, fallopian Sunitinib may increase adverse effects.
tube, or primary peritoneal cancer follow- HERBAL: None significant. FOOD: None
ing initial surgical resection (in combina- known. LAB VALUES: May decrease Hgb,
tion with carboplatin and paclitaxel), then Hct, platelet count, WBC; serum potas-
single-agent bevacizumab. Treatment of sium, sodium. May increase urine protein.
platinum-sensitive ovarian cancer. Treat-
ment of persistent, recurrent, or metastatic AVAILABILITY (Rx)
cervical cancer (in combination with PACL- Injection, Solution: 100 mg/4 mL, 400
itaxel and either CISplatin or topotecan). mg/16 mL vials.

Canadian trade name Non-Crushable Drug High Alert drug


130 bevacizumab

ADMINISTRATION/HANDLING Brain Cancer


B IV
IV: ADULTS, ELDERLY: 10 mg/kg q2wks
(as monotherapy).
b ALERT c Do not give by IV push or Ovarian Cancer (Platinum-Resistant)
bolus. IV: ADULTS, ELDERLY: 10 mg/kg q2wks
Reconstitution • Dilute prescribed with PACLitaxel, DOXOrubicin [liposo-
dose in 100 mL 0.9% NaCl. • Avoid mal], or wkly topotecan or 15 mg/kg
dextrose-containing solutions. • Dis- q3wks (with topotecan q3wks).
card any unused portion.
Rate of administration • Usually Ovarian Cancer (Platinum-Sensitive)
given following other chemotherapy. In- IV: ADULTS, ELDERLY: 15 mg/kg q3wks
fuse initial dose over 90 min. • If first with CARBOplatin/PACLitaxel for 6–8
infusion is well tolerated, second infu- cycles, then 15 mg/kg q3wks as a single
sion may be administered over 60 agent or 15 mg/kg with CARBOplatin/gem-
min. • If 60-min infusion is well toler- citabine for 6–10 cycles, then 15 mg/kg
ated, all subsequent infusions may be q3wks as a single agent. Continue until dis-
administered over 30 min. ease progression or unacceptable toxicity.
Storage • Diluted solution may be
Ovarian Cancer (Following Initial
stored for up to 8 hrs if refrigerated.
Surgery)
IV INCOMPATIBILITIES IV: ADULTS, ELDERLY: 15 mg/kg q3wks
Do not mix with dextrose solutions. with CARBOplatin/PACLitaxel for 6 cycles,
then 15 mg/kg q3wks as a single agent
INDICATIONS/ROUTES/ for total of up to 22 cycles. Continue until
DOSAGE disease progression.
Colorectal Cancer (with Fluorouracil-
Cervical Cancer
Based Chemotherapy)
IV: ADULTS, ELDERLY: 15 mg/kg q3wks
IV: ADULTS, ELDERLY: 5 mg/kg q2wks (in
(in combination with PACLitaxel and either
combination with bolus-IFL) or 10 mg/kg
CISplatin or topotecan). Continue until dis-
q2wks in combination with FOLFOX4).
ease progression or unacceptable toxicity.
Colorectal Cancer Progression (Following
Initial Bevacizumab/Fluorouracil-Based Dose Adjustment for Toxicity
Chemotherapy) Temporary suspension: Mild to mod-
IV: ADULTS, ELDERLY: 5 mg/kg q2wks erate proteinuria, severe hypertension
or 7.5 mg/kg q3wks (in combination not controlled with medical management.
with fluoropyrimidine-irinotecan– or Permanent discontinuation: Wound
fluoropyrimidine-oxaliplatin–based dehiscence requiring intervention, GI
regimen). perforation, hypertensive crises, serious
bleeding, nephrotic syndrome.
Non–Small-Cell Lung Cancer (NSCLC)
IV: ADULTS, ELDERLY: 15 mg/kg q3wks Dosage in Renal/Hepatic Impairment
(in combination with CARBOplatin and No dose adjustment.
PACLitaxel) for 6 cycles.
SIDE EFFECTS
Metastatic Renal Cell Carcinoma Frequent (73%–25%): Asthenia, vomiting,
IV: ADULTS, ELDERLY: 10 mg/kg once anorexia, hypertension, epistaxis, stoma-
q2wks (with interferon alfa). titis, constipation, headache, dyspnea.
Occasional (21%–15%): Altered taste,
dry skin, exfoliative dermatitis, dizziness,
flatulence, excessive lacrimation, skin

underlined – top prescribed drug


bicalutamide 131
discoloration, weight loss, myalgia. Rare
(8%–6%): Nail disorder, skin ulcer, alope- bicalutamide B
cia, confusion, abnormal gait, dry mouth.
bye-ka-loo-ta-mide
ADVERSE EFFECTS/TOXIC (Apo-Bicalutamide , Casodex)
REACTIONS
uCLASSIFICATION
UTI, manifested as urinary frequency/
urgency, proteinuria, occurs frequently. PHARMACOTHERAPEUTIC: Antian-
Most serious adverse effects include HF, drogen hormone. CLINICAL: Anti-
deep vein thrombosis, GI perforation, neoplastic.
wound dehiscence, hypertensive crisis,
nephrotic syndrome, severe hemorrhage.
Anemia, neutropenia, thrombocytopenia USES
occur occasionally. Hypersensitivity reac- Treatment of stage D2 metastatic prostatic
tions occur rarely. May increase risk of carcinoma (in combination with luteiniz-
tracheoesophageal fistula development. ing hormone-releasing hormone [LHRH]
agonist analogues, e.g., leuprolide).
NURSING CONSIDERATIONS Treatment with both drugs must be started
BASELINE ASSESSMENT at same time. OFF-LABEL: Monotherapy
for locally advanced prostate cancer.
Obtain baseline CBC, serum potassium, so-
dium levels at regular intervals during ther- PRECAUTIONS
apy. Assess for proteinuria with urinalysis.
Contraindications: Hypersensitivity to bi­
For pts with 2+ or greater urine dipstick
calutamide. Women, esp. those who are or
reading, a 24-hr urine collection is advised.
may become pregnant. Cautions: Moder-
INTERVENTION/EVALUATION ate to severe hepatic impairment, diabetes.
Monitor B/P regularly for hypertension. As-
ACTION
sess for asthenia. Assist with ambulation if
asthenia occurs. Monitor for fever, chills, Competitively inhibits androgen action by
abdominal pain, epistaxis. Offer antiemetic binding to androgen receptors in target
if nausea, vomiting occurs. Monitor daily tissue. Therapeutic Effect: Prevents
pattern of bowel activity, stool consistency. testosterone stimulation of cell growth in
prostate cancer.
PATIENT/FAMILY TEACHING
• Report abdominal pain, vomiting, con- PHARMACOKINETICS
stipation, headache. • Do not receive im- Well absorbed from GI tract. Protein
munizations without physician’s approval binding: 96%. Metabolized in liver. Ex-
(lowers body’s resistance). • Avoid con- creted in urine and feces. Not removed
tact with anyone who recently received a by hemodialysis. Half-life: 5.8–7 days.
live virus vaccine. • Avoid crowds, those
with infection. • Female pts should take LIFESPAN CONSIDERATIONS
measures to avoid pregnancy during treat- Pregnancy/Lactation: May inhibit
ment. sper­matogenesis in males. Not used in
women. Children: Safety and efficacy
not established. Elderly: No age-related
precautions noted.

Canadian trade name Non-Crushable Drug High Alert drug


132 bictegravir/emtricitabine/tenofovir

INTERACTIONS AST increase over 2 times the upper limit


B DRUG: May increase concentration/ of normal (ULN) or jaundice is noted,
effects of ARIPiprazole, dofetilide, discontinue treatment. Monitor for diar-
lomitapide, nimodipine, warfarin. rhea, nausea, vomiting.
HERBAL: None significant. FOOD: None PATIENT/FAMILY TEACHING
known. LAB VALUES: May increase
• Do not stop taking either medication
serum ALT, AST, alkaline phosphatase,
(both drugs must be continued). • Take
creatinine, bilirubin, BUN, glucose. May
medications at same time each day. • Ex-
decrease WBC, Hgb.
plain possible expectancy of frequent side
AVAILABILITY (Rx) effects. • Report persistent nausea, vomit-
ing, diarrhea, or yellowing of skin or eyes.
Tablets: 50 mg.
ADMINISTRATION/HANDLING
PO
bictegravir/emtri-
• Give without regard to food. • Give citabine/tenofovir
at same time each day.
bik-teg-ra-vir/em-trye-sye-ta-been/
INDICATIONS/ROUTES/DOSAGE ten-oh-foe-veer
Prostatic Carcinoma (Biktarvy)
PO: ADULTS, ELDERLY: 50 mg once daily j BLACK BOX ALERT j Serious,
given concurrently with an LHRH analogue. sometimes fatal lactic acidosis
and severe hepatomegaly with
Dosage in Renal/Hepatic Impairment steatosis (fatty liver) have been
No dose adjustment. reported. Severe exacerbations
of hepatitis B virus (HBV) reported
SIDE EFFECTS in pts co-infected with HIV-1 and
HBV following discontinuation. If
Frequent (49%–10%): Hot flashes, breast discontinuation occurs, monitor
pain, muscle pain, constipation, asthe- hepatic function for at least several
nia, diarrhea, nausea. Occasional (9%– months. Initiate anti-HBV therapy if
8%): Nocturia, abdominal pain, periph- warranted.
eral edema. Rare (7%–3%): Vomiting, Do not confuse bictegravir/
weight loss, dizziness, insomnia, rash, emtricitabine/tenofovir (Bik-
impotence, gynecomastia. tarvy) with elvitegravir/cobi-
cistat/emtricitabine/tenofovir
ADVERSE EFFECTS/TOXIC (Stribild), emtricitabine/rilpi-
REACTIONS virine/tenofovir (Complera),
Sepsis, HF, hypertension, iron deficiency efavirenz/emtricitabine/tenofo-
anemia, interstitial pneumonitis, pulmo- vir (Atripla), or emtricitabine/
nary fibrosis may occur. Severe hepato- tenofovir (Truvada).
toxicity occurs rarely within the first 3–4
mos after treatment initiation. FIXED-COMBINATION(S)
Biktarvy: bictegravir/emtricitabine/
NURSING CONSIDERATIONS tenofovir: 50 mg/200 mg/25 mg.
BASELINE ASSESSMENT uCLASSIFICATION
Obtain baseline CBC, LFT, PSA, serum tes- PHARMACOTHERAPEUTIC: Integrase
tosterone, luteinizing hormone (LH) levels. inhibitor, nucleoside reverse tran-
INTERVENTION/EVALUATION scriptase inhibitor, nucleotide reverse
transcriptase inhibitor. CLINICAL:
Monitor lab studies for changes from Antiretroviral.
baseline. Perform periodic LFT. If ALT,
underlined – top prescribed drug
bictegravir/emtricitabine/tenofovir 133

USES excreted in urine (70%), feces (14%).


Tenofovir excreted in urine feces (32%), B
Indicated as complete regimen for
(less than 1%). Half-life: (bictegravir):
treatment of HIV-1 infection in adults
17 hrs; (emtricitabine): 10 hrs; (tenofo-
who are antiretroviral naïve or to re-
vir): 0.5 hrs.
place the current antiretroviral regimen
in pts who are virologically suppressed LIFESPAN CONSIDERATIONS
(HIV-1 RNA less than 50 copies/mL)
Pregnancy/Lactation: Breastfeeding
on a stable antiretroviral regimen for
not recommended due to risk of post-
at least 3 mos with no history of treat-
natal HIV transmission. Distributed in
ment failure and no known substitu-
breast milk. Children: Safety and efficacy
tions associated with resistance to the
not established. Elderly: Not specified;
individual components of bictegravir/
use caution.
emtricitabine/tenofovir.
PRECAUTIONS INTERACTIONS
DRUG: May significantly increase con-
Contraindications: Hypersensitivity to bi­ct-
centration/effect of dofetilide (contra-
egravir/emtricitabine/tenofovir. Con-
indicated). Rifampin may significantly
comitant use of dofetilide, rifampin.
decrease concentration/effect (contrain-
Cautions: Mild to moderate hepatic/re-
dicated). Carbamazepine, oxcarbaze-
nal impairment. History of depression,
pine, phenobarbital, primidone may
suicidal ideation; hepatitis B or C virus
decrease concentration of tenofovir.
infection. Concomitant use of nephro-
Adefovir, fosphenytoin, phenytoin may
toxic medications. Not recommended in
decrease therapeutic effect of tenofovir.
pts with creatinine clearance less than 30
HERBAL: St. John’s wort may decrease
mL/min; severe hepatic impairment.
concentration/effect of bictegravir, tenofo-
ACTION vir. FOOD: None known. LAB VALUES: May
increase serum amylase, ALT, AST, choles-
Bictegravir inhibits strand transfer activity
terol, creatine kinase, creatinine. May de-
of HIV-1 integrase, essential for viral repli-
crease neutrophils.
cation. Emtricitabine inhibits HIV-1 reverse
transcriptase by competing with natural AVAILABILITY (Rx)
substrates, resulting in chain termination.
Tenofovir inhibits HIV reverse transcrip- Fixed-Dose Combination Tablets: bicte-
tase by interfering with HIV viral RNA- gravir 50 mg/emtricitabine 200 mg/teno-
dependent DNA polymerase. Therapeutic fovir 25 mg.
Effect: Interferes with HIV replication,
slowing progression of HIV infection.
ADMINISTRATION/HANDLING
PO
PHARMACOKINETICS • Give without regard to food. • Admin-
Widely distributed. Bictegravir metabolized ister at least 2 hrs before medications
in liver. Emtricitabine phosphorylated by containing aluminum, calcium, iron, mag-
cellular enzymes. Tenofovir metabolized by nesium (supplements, antacids, laxatives).
enzymatic hydrolysis, mediated by macro-
phages and hepatocytes. Protein binding: INDICATIONS/ROUTES/DOSAGE
(bictegravir): greater than 99%; (emtric- HIV Infection
itabine): less than 4%; (tenofovir): 80%. PO: ADULTS, ELDERLY: 1 tablet once daily.
Peak plasma concentration: (bictegravir):
Dosage in Renal Impairment
2–4 hrs; (emtricitabine): 1.5–2 hrs; (te-
CrCl greater than or equal to 30 mL/
nofovir): 0.5–2 hrs. Bictegravir excreted in
min: No dose adjustment. CrCl less than
feces (60%), urine (35%). Emtricitabine

Canadian trade name Non-Crushable Drug High Alert drug


134 binimetinib
or equal to 30 mL/min: Not recom- INTERVENTION/EVALUATION
B mended. Monitor CD4+ count, viral load, HIV-1
Dosage in Hepatic Impairment RNA level for treatment effectiveness.
Mild to moderate impairment: No Monitor renal function as clinically in-
dose adjustment. Severe impairment: dicated. An increase in serum creatinine
Not recommended. greater than 0.4 mg/dL from baseline
may indicate renal impairment. If dis-
SIDE EFFECTS continuation of drug regimen occurs,
Occasional (6%–2%): Diarrhea, nausea, monitor hepatic function for at least sev-
headache, fatigue, abnormal dreams, eral months. Initiate anti-HBV therapy if
dizziness, insomnia, vomiting, flatulence, warranted. Cough, dyspnea, fever, excess
dyspepsia, abdominal pain, rash. of band cells on CBC may indicate acute
infection (WBC count may be unreliable
ADVERSE EFFECTS/TOXIC in pts with uncontrolled HIV infection).
REACTIONS Screen for immune reconstitution syn-
If therapy is discontinued, pts co-infected drome. Monitor daily pattern of bowel
with hepatitis B virus have an increased activity, stool consistency; I&Os.
risk for viral replication, worsening of
PATIENT/FAMILY TEACHING
hepatic function, and may experience he-
patic decompensation and/or failure. May • Drug resistance can form if therapy is
induce immune reconstitution syndrome interrupted; do not run out of sup-
(inflammatory response to dormant op- ply. • As immune system strengthens, it
portunistic infections, such as Mycobac- may respond to dormant infections hid-
terium avium, cytomegalovirus, PCP, den within the body. Report body aches,
tuberculosis, or acceleration of autoim- chills, cough, fever, night sweats, short-
mune disorders such as Graves’ disease, ness of breath. • Treatment may cause
polymyositis, Guillain-Barré). Acute renal kidney failure. Report flank pain, dark-
failure, Fanconi syndrome (renal tubular ened urine, decreased urine out-
injury with severe hypophosphatemia) put. • Practice safe sex with barrier
were reported. Fatal cases of lactic aci- methods or abstinence. • Lactating fe-
dosis, severe hepatomegaly with steatosis males should not breastfeed.
have occurred. Suicidal ideation, depres-
sion, suicide attempt reported in less than
1% of pts (primarily occurred in pts with
prior psychiatric illness).
binimetinib
NURSING CONSIDERATIONS bin-i-me-ti-nib
(Mektovi)
BASELINE ASSESSMENT Do not confuse binimetinib with
Obtain BUN, serum creatinine, creatinine alectinib, bosutinib, brigatinib,
clearance, GFR; CD4+ count, viral load, cobimetinib, encorafenib, ner-
HIV-1 RNA level; urine glucose, urine pro- atinib or trametinib, or Mektovi
tein. Obtain serum phosphate level in pts with Mekinist.
with chronic kidney disease. Test all pts for uCLASSIFICATION
hepatitis B virus infection. Question history
of depression, suicidal ideation. Receive PHARMACOTHERAPEUTIC: Mitogen-
full medication history (including herbal activated extracellular (MEK) kinase
products); screen for contraindications/ inhibitor. CLINICAL: Antineoplastic.
interactions. Offer emotional support.

underlined – top prescribed drug


binimetinib 135

USES not established. Elderly: No age-related


Treatment of pts with unresectable or precautions noted. B
metastatic melanoma with a BRAF V600E INTERACTIONS
or V600K mutation (in combination with
encorafenib). DRUG: None significant. HERBAL: None
significant. FOOD: None known. LAB
VALUES: May increase serum alkaline
PRECAUTIONS phosphatase, ALT, AST, creatine phospho-
Contraindications: Hypersensitivity to kinase, creatinine, GGT. May decrease
binimetinib. Cautions: Baseline anemia, Hct, Hgb, leukocytes, lymphocytes, neu-
leukopenia, lymphopenia, neutropenia; trophils, RBCs; serum sodium.
pts at risk for hemorrhage (e.g., history of
GI bleeding, coagulation disorders, recent AVAILABILITY (Rx)
trauma; concomitant use of anticoagu- Tablets: 15 mg.
lants, NSAIDs, antiplatelets), hepatic/renal
impairment, pulmonary disease, cardio- ADMINISTRATION/HANDLING
vascular disease, HF. History of thrombo- PO
embolism (deep vein thrombosis [DVT], • Give without regard to food. • If a dose
pulmonary embolism [PE]); pts at risk is missed or vomiting occurs after ad-
for thrombosis (immobility, indwelling ve- ministration, give next dose at regularly
nous catheter/access device, morbid obe- scheduled time. • Do not give a missed
sity, genetic hypercoagulable conditions). dose within 6 hrs of next dose.
ACTION INDICATIONS/ROUTES/DOSAGE
Potent and selective inhibitor of mitogen- Metastatic Melanoma
activated extracellular kinase (MEK) PO: ADULTS, ELDERLY: 45 mg twice daily
pathway. Inhibits MEK1 and MEK2, which (in combination with encorafenib). Con-
are upstream regulators of the ERK path- tinue until disease progression or unac-
way. The ERK pathway promotes cellular ceptable toxicity.
proliferation. MEK1 and MEK2 are part
of the BRAF pathway. Therapeutic Ef- Dose Reduction for Adverse Reactions
fect: Increases apoptosis and reduces First dose reduction: 30 mg twice
tumor growth. daily. Unable to tolerate 30 mg dose:
Permanently discontinue.
PHARMACOKINETICS Dose Modification
Widely distributed. Metabolized in liver. Based on Common Terminology Criteria
Protein binding: 97%. Peak plasma con- for Adverse Events (CTCAE). See pre-
centration: 1.6 hrs. Excreted in feces scribing information for encorafenib for
(62%), urine (31%). Half-life: 3.5 hrs. recommended dose modification. If en-
corafenib is discontinued, binimetinib
LIFESPAN CONSIDERATIONS must also be discontinued.
Pregnancy/Lactation: Avoid preg-
Cardiomyopathy
nancy; may cause fetal harm. Female
Asymptomatic, absolute decrease
pts of reproductive potential should use
in left ventricular ejection fraction
effective contraception during treatment
(LVEF) greater than 10% from base-
and for up to 4 wks after discontinuation.
line and below lower limit of normal
Unknown if distributed in breast milk.
(LLN): Withhold treatment for up to 4
Breastfeeding not recommended during
wks. If LVEF is at or above LLN, and the
treatment and up to 3 days after discon-
decrease from baseline is 10% or less,
tinuation. Children: Safety and efficacy
and pt is asymptomatic, then resume at
Canadian trade name Non-Crushable Drug High Alert drug
136 binimetinib
reduced dose. If LVEF does not recover Rhabdomyolysis, Elevated Serum CPK
B within 4 wks, permanently discontinue. Grade 4 asymptomatic CPK eleva-
Symptomatic HF or absolute de- tion; any CPK elevation with
crease in LVEF of greater than 20% symptoms or with renal impair-
from baseline that is also below ment: Withhold treatment for up to 4
LLN: Permanently discontinue. wks. If improved to Grade 1 or 0, re-
sume at reduced dose. If not resolved
Dermatologic Reactions within 4 wks, permanently discon-
Grade 2 skin reaction: If not im- tinue.
proved within 2 wks, withhold treatment
until improved to Grade 1 or 0. Resume Uveitis
at same dose for first occurrence or re- Grade 1–3 uveitis: Withhold treatment
duce dose if reaction is ­ recurrent. for up to 6 wks if Grade 1 or 2 uveitis
Grade 3 skin reaction: Withhold treat- does not respond to medical therapy or if
ment until improved to Grade 1 or 0. Grade 3 uveitis occurs. If improved, re-
Resume at same dose for first occurrence sume at same dose or reduced dose. If
or reduce dose if reaction is ­recurrent. not improved, permanently discontinue.
Grade 4 skin reaction: Permanently Grade 4 uveitis: Permanently discon-
discontinue. tinue.
Hepatotoxicity Other Adverse Reactions (Including
Grade 2 serum ALT, AST elevation: Hemorrhage)
Maintain dose. If not improved within Any recurrent Grade 2 reaction; first
2 wks, withhold treatment until im- occurrence of any Grade 3 reaction:
proved to Grade 1 or 0 (or to pretreat- Withhold treatment for up to 4 wks. If
ment baseline), then resume at same improved to Grade 1 or 0 (or to pretreat-
dose. Grade 3 or 4 serum ALT, AST ment baseline), resume at reduced dose.
elevation: See Other Adverse Reac- If not improved, permanently discontinue.
tions. First occurrence of any Grade 4 reac-
tion: Permanently discontinue or with-
Ocular Toxicities hold treatment for up to 4 wks. If im-
Symptomatic serious retinopathy; proved to Grade 1 or 0 (or to pretreatment
retinal pigment epithelial detach- baseline), resume at reduced dose. If not
ment: Withhold treatment for up to 10 improved, permanently discontinue. Re-
days. If symptoms improve and become current Grade 3 reaction: Consider
asymptomatic, resume at same dose. If permanent discontinuation. Recurrent
not improved, resume at reduced dose Grade 4 reaction: Permanently discon-
or permanently discontinue. Retinal tinue.
vein occlusion: Permanently discon-
tinue. Thromboembolism
Uncomplicated deep vein thrombo-
Pulmonary Toxicity sis (DVT); pulmonary embolism
Grade 2 interstitial lung disease: (PE): Withhold treatment until improved to
Withhold treatment for up to 4 wks. If Grade 1 or 0, then resume at reduced dose.
improved to Grade 1 or 0, resume at re- Life-threatening PE: Permanently dis-
duced dose. If not resolved within 4 wks, continue.
permanently discontinue. Grade 3 or 4
Dosage in Renal Impairment
interstitial lung disease: Permanently
discontinue. Mild to severe impairment: Not spec-
ified; use caution.

underlined – top prescribed drug


binimetinib 137
Dosage in Hepatic Impairment INTERVENTION/EVALUATION
Mild impairment: No dose adjustment. Monitor CBC for anemia, leukopenia, B
Moderate to severe impairment: lymphopenia, neutropenia; LFT for hepa-
30 mg twice daily. totoxicity (bruising, hematuria, jaundice,
SIDE EFFECTS right upper abdominal pain, nausea, vom-
iting, weight loss); CPK for rhabdomy-
Frequent (43%–20%): Fatigue, nausea, di- olysis (amber-colored urine, flank pain,
arrhea, vomiting, abdominal pain, consti- decreased urine output, muscle aches).
pation, rash, visual impairment. Assess skin for dermal toxicities. Assess
Occasional (18%–13%): Pyrexia, dizzi- for eye pain/redness, visual changes at
ness, peripheral edema. each office visit. Assess LVEF by echo-
ADVERSE EFFECTS/TOXIC cardiogram 1 mo after initiation, then
REACTIONS q2–3mos thereafter during treatment. If
treatment withheld due to change in LVEF,
Anemia, leukopenia, lymphopenia, neu- monitor LVEF q2wks. Monitor for symp-
tropenia is an expected response to toms of DVT (leg or arm pain/swelling),
therapy. Cardiomyopathy reported in 7% PE (chest pain, dyspnea, tachycardia),
of pts. DVT reported in 6% of pts. PE re- HF (dyspnea, peripheral edema, palpita-
ported in 3% of pts. Ocular toxicities in- tions, exercise intolerance). Monitor for
cluding serious retinopathy, retinal de- GI bleeding, bloody stool; symptoms of
tachment, macular edema, retinal vein intracranial bleeding (aphasia, blindness,
occlusion may occur. Uveitis, including confusion, facial droop, hemiplegia, sei-
iritis and iridocyclitis, occurred in 4% of zures). Obtain ABG, radiologic test if in-
pts. Interstitial lung disease, pneumonitis terstitial lung disease or pneumonitis sus-
reported in less than 1% of pts. Grade 3 pected. Diligently screen for infections.
or 4 hepatotoxicity reported in 3%–6%
of pts. Rhabdomyolysis occurs rarely. Se- PATIENT/FAMILY TEACHING
rious hemorrhagic events including GI • Treatment may depress your immune
bleeding, rectal bleeding (4% of pts), system and reduce your ability to fight
hematochezia (3% of pts) may occur. infection. Report symptoms of infection
Fatal intracranial hemorrhage reported such as body aches, chills, cough, fa-
in 2% of pts in the setting of new or pro- tigue, fever. Avoid those with active infec-
gressive brain metastases. Colitis, pan- tion. • Expect frequent cardiac function
niculitis reported in less than 10% of pts. tests, eye exams, skin exams. • Therapy
NURSING CONSIDERATIONS may cause toxic skin reactions, vision
changes, or decrease the heart’s ability to
BASELINE ASSESSMENT pump blood. • Report GI bleeding such
Confirm presence of BRAF V600E or as bloody stools or rectal bleeding. •
V600K mutation in tumor specimen be- Report symptoms of liver problems
fore initiation. Obtain baseline CBC, BMP, (bruising, confusion; amber, dark, or-
LFT, CPK; pregnancy test in female pts of ange-colored urine; right upper abdomi-
reproductive potential. Question history of nal pain, yellowing of the skin or eyes);
cardiovascular disease, genetic hyperco- lung problems (severe cough, difficulty
agulable conditions, hypersensitivity reac- breathing, lung pain, shortness of
tions, HF, pulmonary disease, thrombosis. breath), DVT (swelling, pain, hot feeling
Obtain echocardiogram for LVEF. Screen in the arms or legs; discoloration of ex-
for active infection. Verify use of effective tremity), lung embolism (difficulty
contraception in females of reproductive breathing, chest pain, rapid heart rate),
potential. Offer emotional support. hemorrhagic stroke (confusion, difficulty
speaking, one-sided weakness or paraly-
sis, loss of vision), HF (shortness of
Canadian trade name Non-Crushable Drug High Alert drug
138 bisoprolol
breath, palpitations; swelling of legs, an- ACTION
B kle, feet); rhabdomyolysis (dark-colored Selectively blocks beta1-adrenergic re-
urine, decreased urinary output, fatigue, ceptors. Therapeutic Effect: Slows
muscle aches). • Report any vision sinus heart rate, decreases B/P.
changes, eye redness. • Avoid pregnancy.
Female pts of childbearing potential PHARMACOKINETICS
should use effective contraception during Well absorbed from GI tract. Protein
treatment and for at least 4 wks after last binding: 26%–33%. Metabolized in liver.
dose. Do not breastfeed. Primarily excreted in urine. Not removed
by hemodialysis. Half-life: 9–12 hrs
(increased in renal impairment).
bisoprolol LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Readily crosses
bi-soe-proe-lol placenta; distributed in breast milk. Avoid
(Apo-Bisoprolol , Novo-Bisopro- use during first trimester. May produce
lol ) bradycardia, apnea, hypoglycemia, hypo-
Do not confuse bisoprolol with thermia during delivery, low-birth-weight
metoprolol. infants. Children: Safety and efficacy
not established. Elderly: Age-related
FIXED-COMBINATION(S)
peripheral vascular disease may increase
Ziac: bisoprolol/hydroCHLOROthia- risk of decreased peripheral circulation.
zide (a diuretic): 2.5 mg/6.25 mg,
5 mg/6.25 mg, 10 mg/6.25 mg. INTERACTIONS
DRUG: Alpha2 agonists (e.g., cloNI-
uCLASSIFICATION
Dine) may increase AV-blocking effect.
PHARMACOTHERAPEUTIC: Beta 1 Strong CYP3A4 inducers (e.g., carBA-
selective adrenergic blocker. CLINI- Mazepine, phenytoin, rifAMPin) may
CAL: Antihypertensive. decrease concentration/effect. Droneda-
rone, fingolimod, rivastigmine may
increase bradycardic effect. May increase
USES vasoconstriction of ergot derivatives
Management of hypertension, alone or (e.g., dihydroergotamine, ergota-
in combination with other medications. mine). HERBAL: Herbals with hy-
OFF-LABEL: Chronic stable angina pecto- pertensive properties (e.g., licorice,
ris, premature ventricular contractions, yohimbe) or hypotensive properties
supraventricular arrhythmias, HF. (e.g., garlic, ginger, ginkgo biloba)
may alter effects. St John’s wort may de-
PRECAUTIONS crease concentration/effect. FOOD: None
Contraindications: Hypersensitivity to known. LAB VALUES: May increase ANA
bisoprolol. Cardiogenic shock, marked titer, serum BUN, creatinine, potassium,
sinus bradycardia, overt HF, second- or uric acid, lipoproteins, triglycerides.
third-degree heart block (except in pts with
pacemaker). Cautions: Concurrent use of AVAILABILITY (Rx)
digoxin, verapamil, diltiaZEM, HF, history Tablets: 5 mg, 10 mg.
of severe anaphylaxis to allergens, renal/
hepatic impairment, hyperthyroidism, dia- ADMINISTRATION/HANDLING
betes, bronchospastic disease, myasthenia PO
gravis, psychiatric disease, peripheral vas- • Give without regard to food.
cular disease, Raynaud’s disease.

underlined – top prescribed drug


bivalirudin 139
INDICATIONS/ROUTES/DOSAGE PATIENT/FAMILY TEACHING
Hypertension • Do not abruptly discontinue medica- B
PO: ADULTS, ELDERLY: Initially, 2.5–5 tion. • Compliance with therapy regimen
mg once daily. May increase to 10 mg, is essential to control hypertension. • If
then to 20 mg once daily. Usual dose: dizziness occurs, sit or lie down immedi-
5–10 mg once daily. ately. • Avoid tasks that require alertness,
motor skills until response to drug is estab-
Dosage in Renal Impairment lished. • Take pulse properly before each
CrCl less than 40 mL/min: ADULTS, dose and report excessively slow pulse rate
ELDERLY: Initially, give 2.5 mg. (less than 60 beats/min). Report numbness
of extremities, dizziness. • Do not use
Dosage in Hepatic Impairment nasal decongestants, OTC cold prepara-
Cirrhosis, hepatitis: Initially, 2.5 mg. tions (stimulants) without physician’s ap-
proval. • Restrict salt, alcohol intake.
SIDE EFFECTS
Frequent (11%–8%): Fatigue, headache.
Occasional (4%–2%): Dizziness, arthral-
gia, peripheral edema, URI, rhinitis, phar- bivalirudin
yngitis, diarrhea, nausea, insomnia. Rare
(less than 2%): Chest pain, asthenia, dys- bye-val-i-rue-din
pnea, vomiting, bradycardia, dry mouth, (Angiomax)
diaphoresis, decreased libido, impotence.
uCLASSIFICATION
ADVERSE EFFECTS/
PHARMACOTHERAPEUTIC: Direct
TOXIC REACTIONS
thrombin inhibitor. CLINICAL: Anti-
Overdose may produce profound brady- coagulant.
cardia, hypotension. Abrupt withdrawal
may result in diaphoresis, palpitations,
headache, tremors. May precipitate HF, MI USES
in pts with cardiac disease, thyroid storm in Anticoagulant in pts undergoing percuta-
pts with thyrotoxicosis, peripheral ischemia neous transluminal coronary angioplasty
in those with existing peripheral vascular (PTCA) in conjunction with aspirin and
disease. Hypoglycemia may occur in previ- provisional glycoprotein llb/llla inhibitor.
ously controlled diabetes. Thrombocytope- Pts with heparin-induced thrombocyto-
nia, unusual bruising/bleeding occur rarely. penia (HIT) and thrombosis syndrome
NURSING CONSIDERATIONS (HITTS) while undergoing percutaneous
coronary intervention (PCI) (in conjunc-
BASELINE ASSESSMENT tion with aspirin). OFF-LABEL: HIT; ST-
Assess baseline renal/hepatic function tests. segment elevation MI (STEMI) undergoing
Assess B/P, apical pulse immediately before PCI.
drug is administered (if pulse is 60/min or
less or systolic B/P is less than 90 mm Hg, PRECAUTIONS
withhold medication, contact physician). Contraindications: Hypersensitivity to bi­
valirudin. Active major bleeding. Cau-
INTERVENTION/EVALUATION tions: Renal impairment, conditions as-
Monitor B/P, pulse for quality, irregular rate, sociated with increased risk of bleeding
bradycardia. Assist with ambulation if dizzi- (e.g., bacterial endocarditis, recent ma-
ness occurs. Assess for peripheral edema. jor bleeding, CVA, stroke, intracerebral
Monitor daily pattern of bowel activity, stool surgery, hemorrhagic diathesis, severe
consistency. Assess neurologic status. hypertension, severe renal/hepatic im-
pairment, recent major surgery).

Canadian trade name Non-Crushable Drug High Alert drug


140 bivalirudin
ACTION solved. • Dilute each vial in 50 mL D5W
B Acts as a specific and reversible direct or 0.9% NaCl bag to yield final concen-
thrombin inhibitor by binding to its re- tration of 5 mg/mL (1 vial in 50 mL, 2
ceptor sites. Therapeutic Effect: Pre- vials in 100 mL, 5 vials in 250 mL). • If
vents thrombin-mediated cleavage of low-rate infusion is used after initial infu-
fibrinogen to fibrin and activates factors sion, reconstitute the 250-mg vial with
V, VIII and XIII. added 5 mL Sterile Water for Injec-
tion. • Gently swirl until fully dis-
PHARMACOKINETICS solved. • Dilute each vial in 500 mL
Route Onset Peak Duration D5W or 0.9% NaCl bag to yield final
IV Immediate N/A 1 hr
concentration of 0.5 mg/mL. • Pro-
duces a clear, colorless solution (do not
Primarily eliminated by kidneys. Twenty- use if cloudy or contains a precipitate).
five percent removed by hemodialysis. Rate of administration • Adjust IV in-
Half-life: 25 min (increased in moder- fusion based on aPTT or pt’s body weight.
ate to severe renal impairment). Storage • Store unreconstituted vials
at room temperature. • Reconstituted
LIFESPAN CONSIDERATIONS solution may be refrigerated for up to 24
Pregnancy/Lactation: Unknown if drug hrs. • Final dilution with a concentra-
crosses placenta or is distributed in breast tion of 0.5–5 mg/mL is stable at room
milk. Children: Safety and efficacy not temperature for up to 24 hrs.
established. Elderly: Age-related renal im-
pairment may require dosage adjustment. IV INCOMPATIBILITIES
Alteplase (Activase), amiodarone (Cord-
INTERACTIONS arone), amphotericin B (AmBisome,
DRUG: Anticoagulants (e.g., heparin, Abelcet), diazePAM (Valium), DOBUTa-
warfarin), antiplatelets (e.g., aspirin, mine (Dobutrex), reteplase (Retavase),
clopidogrel), NSAIDs (e.g., diclofenac, streptokinase (Streptase), vancomycin
ibuprofen, naproxen), thrombolytic (Vancocin).
therapy (e.g., TPA) may increase risk of
bleeding. Apixaban, dabigatran, edoxa- IV COMPATIBILITIES
ban, rivaroxaban may enhance antico- Refer to IV compatibility chart in front of
agulant effect. Vorapaxar may increase book.
adverse ­effects. HERBAL: Herbals with
anticoagulant/antiplatelet properties INDICATIONS/ROUTES/DOSAGE
(e.g., feverfew, garlic, ginger, ginkgo Anticoagulant in Pts with Unstable
biloba) may enhance effects. FOOD: None Angina, HIT, or HITTS Undergoing PTCA
known. LAB VALUES: Prolongs activated IV: ADULTS, ELDERLY: 0.75 mg/kg as IV
partial thromboplastin time (aPTT), pro- bolus, followed by IV infusion at rate of
thrombin time (PT). 1.75 mg/kg/hr for duration of procedure
and up to 4 hrs postprocedure. IV infu-
AVAILABILITY (Rx) sion may be continued beyond initial 4 hrs
Injection, Powder for Reconstitution: 250 at rate of 0.2 mg/kg/hr for up to 20 hrs.
mg.
Dosage in Renal Impairment
ADMINISTRATION/HANDLING b ALERT c Initial bolus dose remains
unchanged.
IV
Creatinine Clearance Dosage
Reconstitution • To each 250-mg vial 30 mL/min or greater 1.75 mg/kg/hr
add 5 mL Sterile Water for Injec- 10–29 mL/min 1 mg/kg/hr
tion. • Gently swirl until fully dis- Dialysis 0.25 mg/kg/hr

underlined – top prescribed drug


blinatumomab 141

Dosage in Hepatic Impairment


USES
Treatment of Philadelphia chromosome- B
No dosage adjustment.
negative relapsed or refractory B-cell
SIDE EFFECTS precursor acute lymphoblastic leukemia
Frequent (42%): Back pain. Occasional (ALL) in adults and children. Treatment
(15%–12%): Nausea, headache, hypoten- of B-cell precursor ALL in first or second
sion, generalized pain. Rare (8%–4%): In- complete remission with minimal resid-
jection site pain, insomnia, hypertension, ual disease.
anxiety, vomiting, pelvic or abdominal
pain, bradycardia, nervousness, dyspep- PRECAUTIONS
sia, fever, urinary retention. Contraindications: Hypersensitivity to
blinatumomab. Cautions: Baseline ane-
ADVERSE EFFECTS/TOXIC mia, leukopenia, neutropenia, throm-
REACTIONS bocytopenia; active infection or pts at
Hemorrhagic events occur rarely, charac- increased risk of infection (diabetes,
terized by significant fall in B/P or Hgb/Hct. indwelling catheters), hepatic/renal
­impairment, electrolyte imbalance, high
NURSING CONSIDERATIONS tumor burden, history of cognitive or sei-
zure disorders, syncope, elderly.
BASELINE ASSESSMENT
Assess CBC, PT/INR, aPTT, renal function. ACTION
Determine initial B/P. Binds to CD19 expressed on B cells
INTERVENTION/EVALUATION and CD3 expressed on T cells. Activates
endogenous T cells, forming a cytolytic
Monitor aPTT, CBC, urine and stool spec- synapse between a cytotoxic T cell and the
imen for occult blood, renal function cancer target B cell. Therapeutic Effect:
studies. Monitor for evidence of bleed- Inhibits tumor cell growth and metastasis
ing. Assess for decrease in B/P, increase in ALL.
in pulse rate. Question for increase in
vaginal bleeding during menses. PHARMACOKINETICS
Widely distributed. Metabolism not speci-
blinatumomab fied; degrades into small peptides and
amino acids via catabolic pathway. Pro-
blin-a-toom-oh-mab tein binding: Not specified. Steady state
(Blincyto) reached within 24 hrs. Excretion not
j BLACK BOX ALERT jCytokine specified; negligible amounts excreted in
release syndrome (CRS) or neuro- urine. Half-life: 2.1 hrs.
logic toxicities, which may be life
threatening or fatal, have occurred. LIFESPAN CONSIDERATIONS
Interrupt or discontinue treatment
as recommended. Pregnancy/Lactation: May cause fe-
Do not confuse blinatumomab tal harm. Avoid pregnancy. Unknown if
with ibritumomab or tositu- distributed in breast milk. Must either
momab. discontinue drug or discontinue breast-
feeding. Children: Safety and efficacy
uCLASSIFICATION not established. Elderly: May have
PHARMACOTHERAPEUTIC: Anti- increased risk of neurologic toxicities,
CD19/CD3 bispecific T-cell engager. including cognitive disorder, encepha-
Monoclonal antibody. CLINICAL: An- lopathy, confusion, seizure; serious infec-
tineoplastic. tions, hepatic impairment.

Canadian trade name Non-Crushable Drug High Alert drug


142 blinatumomab

INTERACTIONS Rate of administration • Administer


B DRUG: May decrease therapeutic ef- as continuous IV infusion at a constant
fect of BCG (intravesical), vaccines flow rate using an infusion pump. The
(live). May increase adverse effects pump should be programmable, lock-
of natalizumab, vaccines (live). able, nonelastomeric, and have an
HERBAL: Echinacea may decrease thera- alarm. • Infusion bags should be in-
peutic effect. FOOD: None known. LAB fused over 24–48 hrs. Infuse the total
VALUES: May decrease immunoglobu- 240-mL solution according to the in-
lins, Hgb, Hct, neutrophils, leukocytes, structions on the pharmacy label of the
platelets; serum albumin, magnesium, bag at one of the following constant rates:
phosphate, potassium. May increase se- 10 mL/hr over 24 hrs, or 5 mL/hr over
rum ALT, AST, bilirubin, GGT, glucose; 48 hrs. • Infuse via dedicated
body weight. line. • Use sterile, nonpyrogenic, low
protein-binding, 0.2-micron in-line filter.
AVAILABILITY (Rx) Storage • Refrigerate unused vials
Injection, Lyophilized Powder for Recon- and IV solution stabilizer until time of
stitution: 35 mcg/vial. use. • Protect from light. • Do not
freeze. • Reconstituted vials may be
ADMINISTRATION/HANDLING stored at room temperature up to 4 hrs
or refrigerated up to 24 hrs. • Pre-
IV pared IV bag solutions may be stored at
• Hospitalization is recommended for the room temperature up to 48 hrs or refrig-
first 9 days of the first cycle and the first 2 erated up to 8 days. • If prepared IV
days of the second cycle. For all subsequent bag solution is not administered with the
cycle starts and reinitiation (e.g., if treat- infusion time frame and temperature
ment is interrupted for 4 or more hrs), indicated, it must be discarded; do not
supervision by a healthcare professional or refrigerate again.
hospitalization is recommended. • Do
INDICATIONS/ROUTES/DOSAGE
not flush infusion line after administration,
esp. when changing infusion bags. Flushing Note: See Administration/Handling.
of infusion line can result in excess dosage
Acute Lymphoblastic Leukemia (ALL)
and complications. • At end of infusion,
IV: ADULTS, ELDERLY, CHILDREN: A treat-
any used solution in IV bag and IV lines
ment course consists of up to 2 cycles
should be disposed of in accordance with
for induction followed by 3 additional
local requirements.
cycles for consolidation and up to 4 addi-
Premedication • Premedicate with
tional cycles of continued therapy. Cycles
dexamethasone 20 mg IV 1 hr prior to
1–5 consist of 4 wks of continuous IV
the first dose of each cycle, prior to step
infusion followed by a 2-wk treatment-
dose (such as cycle 1 on day 8), or when
free interval. Cycles 6–9 consist of 4
restarting an infusion after an interrup-
wks of continuous IV infusion followed
tion of 4 or more hrs.
by an 8-wk treatment-free interval. PTS
Reconstitution • Reconstitution
WEIGHING 45 KG OR MORE: (Induction
guidelines are highly specific. Infusion
cycle 1): Administer 9 mcg/day on days
bags must be prepared by personnel
1–7, then at 28 mcg/day on days 8–28
trained in aseptic preparations and ad-
as continuous infusion. (Induction cycle
mixing of oncologic drugs following strict
2, consolidation cycles 3–5, continued
environmental specifications at a USP
therapy cycles 6–9): Administer 28 mcg/
797 compliant facility using ISO Class 5
day on days 1–28. PTS WEIGHING LESS
laminar flow hood or better. • See
THAN 45 KG: (Cycle 1): 5 mcg/m2/day
manufacturer guidelines for details.
(not to exceed 9 mcg/day) on days 1–7

underlined – top prescribed drug


blinatumomab 143
and 15 mcg/m2/day (Maximum: 28 mcg/day. Increase dose to 28 mcg/day
mcg/day) on days 8–28 as continuous after 7 days if toxicity does not recur. If B
infusion. (Induction cycle 2, consolida- toxicity takes more than 14 days to re-
tion cycles 3–5, continued therapy cycles solve, permanently discontinue. CTCAE
6–9): Administer 15 mcg/m2/day (Maxi- Grade 4: Consider permanent discon-
mum: 28 mcg/day) on days 1–28. tinuation.
Elevated Hepatic Enzymes
Acute Lymphoblastic Leukemia, Minimal Interrupt treatment if ALT/AST rise to
Residual Disease (MRD)–Positive greater than 5 times upper limit of normal
IV: ADULTS, ELDERLY, CHILDREN: A treat- (ULN) or bilirubin rises to more than 3
ment course consists of 1 induction cycle times ULN. Consider dose recommendation
followed by up to 3 additional cycles for as listed in other clinically relevant adverse
consolidation. Each cycle consists of 4 reactions or as ordered by prescriber.
wks of continuous infusion followed by a
2-wk treatment-free interval. PTS WEIGH- Dosage in Renal Impairment
ING 45 KG OR MORE: Administer 28 mcg/ CrCl equal to or greater than 30
day on days 1–28. PTS WEIGHING LESS mL/min: No dose adjustment. CrCl
THAN 45 KG: Administer 15 mcg/m2/day less than 30 mL/min or hemodialy-
(Maximum: 28 mcg/day) on days 1–28. sis: Not specified; use caution.

Dose Modification Dosage in Hepatic Impairment


Based on Common Terminology Criteria for Not specified; use caution. Hepatic toxicity
Adverse Events (CTCAE). Note: If interrup- during treatment: see dose modification.
tion after an adverse event is no longer than
7 days, continue the same cycle to a total of SIDE EFFECTS
28 days of infusion inclusive of the days be- Frequent (62%–36%): Pyrexia, head-
fore and after the interruption in that cycle. ache. Occasional (25%–5%): Peripheral
If interruption due to an adverse event is edema, nausea, tremor, constipation, di-
longer than 7 days, start new cycle. arrhea, cough, fatigue, dyspnea, insom-
Cytokine Release Syndrome nia, chills, abdominal pain, dizziness,
CTCAE Grade 3: Withhold until re- back pain, extremity pain, vomiting, bone
solved, then restart at 9 mcg/day. In- pain, chest pain, decreased appetite,
crease dose to 28 mcg/day after 7 days arthralgia, hypotension, hypertension,
if toxicity does not occur. CTCAE Grade tachycardia, confusion, paresthesia. Rare
4: Permanently discontinue. (4%–2%): Aphasia, memory impairment.
Neurological Toxicity
CTCAE Grade 3: Withhold until no ADVERSE EFFECTS/TOXIC
more than Grade 1 for at least 3 days, then REACTIONS
restart at 9 mcg/day. Increase dose to 28 Myelosuppression (principally, anemia,
mcg/day after 7 days if toxicity does not re- leukopenia, neutropenia, thrombocyto-
cur. If toxicity occurred at 9 mcg/day, or if penia) is an expected outcome of treat-
toxicity takes more than 7 days to resolve, ment. Cytokine release syndrome (CRS)
permanently discontinue. CTCAE Grade may be life threatening or fatal. Symptoms
4: Permanently discontinue. of CRS may include asthenia, hypoten-
Seizure sion, nausea, pyrexia; elevated ALT/AST,
Permanently discontinue if more than bilirubin; disseminated intravascular co-
one seizure occurs. agulation (DIC), capillary leak syndrome,
Other Clinically Relevant Adverse hemophagocytic lymphohistiocytosis/mac-
Reactions rophage activation syndrome (HLH/MAS).
CTCAE Grade 3: Withhold until no Infusion reactions have occurred and may
more than Grade 1, then restart at 9 be clinically indistinguishable from CRS.

Canadian trade name Non-Crushable Drug High Alert drug


144 bortezomib
Neurologic toxicities such as altered level PATIENT/FAMILY TEACHING
B of consciousness, balance disorders, con- • Treatment may cause life-threatening
fusion, disorientation encephalopathy, sei- side effects that must be immediately
zures, speech disorders, syncope occurred treated by medical personnel. • Report
in approx. 50% of pts and may affect abil- symptoms of cytokine release syndrome,
ity to drive or operate machinery. Median such as chills, facial swelling, fever, low
time to onset of neurologic toxicity was 7 blood pressure, nausea, vomiting, weak-
days. CTCAE Grade 3 toxicities or higher ness; any infusion-related reactions, such
occurred in 15% of pts. Serious infections as difficulty breathing or skin rash. • Re-
such as opportunistic infections, bacterial/ port any neurologic problems, such as
viral/fungal infections, sepsis, pneumo- confusion, difficulty speaking or slurred
nia, catheter-site infections occurred in speech, loss of consciousness, loss of bal-
25% of pts. Other life-threatening or fatal ance, or seizures. • Treatment may
events may include tumor lysis syndrome, lower your white blood cell count and
neutropenia/febrile neutropenia, leuko- increase your risk of infection. Report any
encephalopathy. Medication preparation signs of infection, such as fever, cough,
and administration errors have occurred, fatigue, or burning with urination. Keep
resulting in underdose or overdose. Im- area around IV catheter clean at all times
munogenicity (anti-blinatumomab anti- to reduce risk of infection. • Do not
bodies) occurred in less than 1% of pts. change or alter settings on infusion
pump, even if the pump alarm sounds.
NURSING CONSIDERATIONS Any changes made to the infusion pump
BASELINE ASSESSMENT by anyone other than trained medical
Obtain baseline CBC, BMP, LFTs, serum personnel can result in a dose that is too
magnesium, phosphate, ionized calcium, high or too low and may be life threaten-
vital signs. Consider electrolyte correc- ing. • Report symptoms of liver prob-
tion before starting treatment. Screen lems, such as bruising, confusion, dark
for home medications requiring narrow or amber-colored urine, right upper ab-
therapeutic index. Screen for active in- dominal pain, or yellowing of the skin or
fection, history of seizures, hepatic/renal eyes. • Avoid tasks that require alert-
impairment, cognitive disorders. Verify ness, motor skills until response to drug
pregnancy status in women of childbear- is established. Do not drive or operate
ing potential. Assess plans of breastfeed- machinery. • Blood levels will be moni-
ing. Conduct full neurologic assessment. tored routinely. • Hospitalization is re-
quired when starting therapy.
INTERVENTION/EVALUATION
Monitor CBC, LFTs, serum electrolytes
(correct as indicated), vital signs. Moni- bortezomib
tor closely for cytokine release syndrome,
neurologic toxicities, serious infection, bor-tez-oh-mib
tumor lysis syndrome, hepatic impair- (Velcade)
ment. Keep area around IV site clean to uCLASSIFICATION
reduce risk of infection. Do not adjust
setting of infusion pump. Pump changes PHARMACOTHERAPEUTIC: Protea-
may result in dosing errors. Do not flush some inhibitor. CLINICAL: Antineo-
IV line after infusion completion. Initiate plastic.
fall precautions. Monitor I&O.
USES
Treatment of relapsed or refractory
mantle cell lymphoma. Treatment of mul-

underlined – top prescribed drug


bortezomib 145
tiple myeloma. OFF-LABEL: Treatment of ADMINISTRATION/HANDLING
Waldenström’s macroglobulinemia; pe- B
ripheral or cutaneous T-cell lymphoma; IV
systemic light-chain amyloidosis. Reconstitution • Reconstitute vial with
3.5 mL 0.9% NaCl to provide a concentra-
PRECAUTIONS
tion of 1 mg/mL.
Contraindications: Hypersensitivity to bort- Rate of administration • Give as bo-
ezomib, boron or mannitol; intrathecal ad- lus IV injection over 3–5 sec.
ministration. Cautions: Concomitant use Storage • Store unopened vials at room
of CYP3A4 inhibitors, history of syncope, temperature. • Once reconstituted, solu-
concomitant use of antihypertensives; de- tion may be stored at room temperature
hydration, diabetes, hepatic impairment, for up to 3 days or for 5 days if refrigerated.
preexisting cardiac disease, neuropathy.
SQ
ACTION Reconstitution • Reconstitute vial
Inhibits proteasomes (enzyme complexes with 1.4 mL 0.9% NaCl to provide a con-
regulating protein homeostasis within the centration of 2.5 mg/mL.
cell). Therapeutic Effect: Produces
cell-cycle arrest, apoptosis. INDICATIONS/ROUTES/DOSAGE
Mantle Cell Lymphoma (Initial Treatment)
PHARMACOKINETICS IV: ADULTS, ELDERLY: 1.3 mg/m2 days 1, 4,
Widely distributed. Protein binding: 83%. 8, 11 of a 21-day cycle for 6 cycles (in
Primarily metabolized by enzymatic ac- combination with riTUXimab, cyclophos-
tion. Significant biliary excretion, with phamide, DOXOrubicin, and predniSONE).
lesser amount excreted in urine. Half- If response is seen at cycle 6, may continue
life: 9–15 hrs. for 2 additional cycles.
LIFESPAN CONSIDERATIONS Mantle Cell Lymphoma (Relapsed)
Pregnancy/Lactation: May induce de- IV, SQ: ADULTS, ELDERLY:Treatment cycle
generative effects in ovary, degenerative consists of 1.3 mg/m2 twice wkly on days 1,
changes in testes. May affect male/female 4, 8, and 11 for 2 wks of a 21-day treatment
fertility. Breastfeeding not recommended. for 8 cycles. Therapy extending beyond 8
Children: Safety and efficacy not estab- cycles may be given by standard schedule.
lished. Elderly: Increased incidence of
Multiple Myeloma (Initial Treatment)
Grade 3 or 4 thrombocytopenia.
IV, SQ: ADULTS, ELDERLY: (with mel-
INTERACTIONS phalan and predniSONE) 1.3 mg/m2 on days
1, 4, 8, 11, 22, 25, 29, 32 of a 42-day cycle for
DRUG: CYP3A4 inhibitors (e.g., itra-
4 cycles, then 1.3 mg/m2 on days 1, 8, 22, 29
conazole, ketoconazole) may increase
of a 42-day cycle for 5 cycles.
concentration/toxicity. CYP3A4 inducers
(e.g., rifAMPin) may decrease concen- Multiple Myeloma (Relapsed)
tration/effect (avoid use). HERBAL: Green IV, SQ: ADULTS, ELDERLY: 1.3 mg/m2
tea, green tea extracts may diminish twice wkly for 2 wks on days 1, 4, 8, 11
effect. St. John’s wort may decrease of a 21-day treatment cycle for 8 cycles.
level/effect. FOOD: Grapefruit products Therapy extending beyond 8 cycles may
may increase concentration. LAB VAL- be given once wkly for 4 wks followed by
UES: May significantly decrease WBC, a 13-day rest period.
Hgb, Hct, platelet count, neutrophils.
Dosage Adjustment Guidelines
AVAILABILITY (Rx) Withhold therapy at onset of CTCAE Grade
Injection, Powder for Reconstitution: 3.5 mg. 3 nonhematologic or Grade 4 hemato-

Canadian trade name Non-Crushable Drug High Alert drug


146 bosutinib
logic toxicities, excluding neuropathy. NURSING CONSIDERATIONS
B When symptoms resolve, resume therapy
at a 25% reduced dosage. BASELINE ASSESSMENT
Obtain baseline CBC. Ensure adequate
Dosage Adjustment Guidelines with
hydration prior to initiation of therapy.
Neuropathic Pain, Peripheral Sensory
Antiemetics, antidiarrheals may be effec-
Neuropathy
tive in preventing, treating nausea, vomit-
For CTCAE Grade 1 toxicity with pain or ing, diarrhea.
Grade 2 (interfering with function but not
activities of daily living [ADL]), 1 mg/m2. INTERVENTION/EVALUATION
For Grade 2 toxicity with pain or Grade Routinely assess B/P; monitor pt for or-
3 (interfering with ADL), withhold drug thostatic hypotension. Maintain strict
until toxicity is resolved, then reinitiate I&O. Monitor CBC, esp. platelet count,
with 0.7 mg/m2. For Grade 4 toxicity throughout treatment. Monitor renal,
(permanent sensory loss that interferes hepatic, pulmonary function throughout
with function), discontinue bortezomib. therapy. Encourage adequate fluid intake
Dosage in Renal Impairment
to prevent dehydration. Monitor tem-
No dose adjustment. perature and be alert to high potential for
fever. Monitor for peripheral neuropathy
Dosage in Hepatic Impairment (burning sensation, neuropathic pain,
Mild impairment: No initial adjustment. paresthesia, hyperesthesia). Avoid IM in-
Moderate (bilirubin greater than 1.5–3 jections, rectal temperatures, other trau-
times upper limit of normal [ULN]) to mas that may induce bleeding.
severe (bilirubin greater than 3 times PATIENT/FAMILY TEACHING
ULN) impairment: Decrease initial dose
to 0.7 mg/m2 (based on tolerance may in- • Report new/worsening vomiting,
crease to 1 mg/m2 or decrease to 0.5 mg/m2). bruising/bleeding, breathing difficul-
ties. • Discuss importance of preg-
SIDE EFFECTS nancy testing, avoidance of pregnancy,
Expected (65%–36%): Fatigue, malaise, measures to prevent pregnancy. • In-
asthenia, nausea, diarrhea, anorexia, con- crease fluid intake. • Avoid tasks that
stipation, fever, vomiting. Frequent (28%– require mental alertness, motor skills
21%): Headache, insomnia, arthralgia, until response to drug is established.
limb pain, edema, paresthesia, dizziness,
rash. Occasional (18%–11%): Dehydra-
tion, cough, anxiety, bone pain, muscle bosutinib
cramps, myalgia, back pain, abdominal
pain, taste alteration, dyspepsia, pruritus, boe-sue-ti-nib
hypotension (including orthostatic hypo- (Bosulif)
tension), rigors, blurred vision.
uCLASSIFICATION
ADVERSE EFFECTS/TOXIC PHARMACOTHERAPEUTIC: BCR-ABL
REACTIONS tyrosine kinase inhibitor. CLINI-
Thrombocytopenia occurs in 40% of pts. CAL: Antineoplastic.
GI, intracerebral hemorrhage are associ-
ated with drug-induced thrombocytope-
nia. Anemia occurs in 32% of pts. New USES
onset or worsening of existing n­ europathy Treatment of chronic, accelerated, or
occurs in 37% of pts. Symptoms may im- blast phase Philadelphia chromosome–
prove in some pts upon drug discontinua- positive chronic myelogenous leukemia
tion. Pneumonia occurs occasionally. (Ph+CML) with resistance or intolerance

underlined – top prescribed drug


bosutinib 147
to prior therapy. Treatment of newly diag- phenytoin, PHENobarbital), moder-
nosed chronic phase Ph+CML. ate CYP3A4 inducers (e.g., bosentan, B
nafcillin, modafinil) may decrease
PRECAUTIONS concentration/effect. Proton pump in-
Contraindications: Hypersensitivity to hibitors (e.g., omeprazole, panto-
bo­sutinib. Cautions: Baseline anemia, prazole) may reduce absorption, con-
thrombocytopenia, neutropenia; hepatic centration. HERBAL: St. John’s wort may
impairment, recent diarrhea, pulmonary decrease effectiveness. Bitter orange,
edema, HF, fluid retention. Pts with his- pomegranate, star fruit may increase
tory of pancreatitis, moderate to severe concentration/effect. FOOD: Grapefruit
renal impairment. Avoid concurrent use products may decrease bosutinib con-
of CYP3A4 inducers/inhibitors. centration. LAB VALUES: May decrease
Hgb, platelets, WBCs, serum phosphorous.
ACTION May increase serum ALT, AST, bilirubin, li-
Inhibits Bcr-Abl tyrosine kinase, a trans- pase.
location-created enzyme, created by the
Philadelphia chromosome abnormality AVAILABILITY (Rx)
noted in chronic myelogenous leukemia Tablets: 100 mg, 400 mg, 500 mg.
(CML). Inhibits Src-family kinase, in-
cluding Src, Lyn, and Hck. Therapeutic ADMINISTRATION/HANDLING
Effect: Inhibits tumor cell growth and PO
proliferation in chronic, accelerated, or • Give with food. Do not break, crush,
blast phase CML. dissolve, or divide tablets.
PHARMACOKINETICS INDICATIONS/ROUTES/DOSAGE
Well absorbed following oral administra- Ph+CML (Resistant or Intolerant to Prior
tion. Protein binding: 94%. Metabolized Therapy)
in liver. Excreted in feces (91%), urine PO: ADULTS, ELDERLY: 500 mg once
(3%). Half-life: 22.5 hrs. daily. Continue until disease progression
or unacceptable toxicity. If complete he-
LIFESPAN CONSIDERATIONS matologic response not achieved by wk
Pregnancy/Lactation: Potential for 8 or complete cytogenetic response not
embryo/fetal toxicity. Avoid pregnancy. achieved by wk 12, in absence of Grade
Must use effective contraception during 3 or higher adverse reactions, may in-
treatment and for at least 30 days after crease to 600 mg once daily.
treatment. Unknown if distributed in
breast milk. Avoid breastfeeding. Chil- Ph+CML (Newly Diagnosed Chronic Phase)
dren: Safety and efficacy not established. PO: ADULTS, ELDERLY: 400 mg once daily.
Elderly: No age-related precautions Continue until disease progression or un-
noted. acceptable toxicity.
INTERACTIONS CML with Baseline Renal Impairment
DRUG: Strong CYP3A inhibitors and/ Ph+CML (intolerant): CrCl less than 30
or P-glycoprotein (P-gp) inhibitors mL/min: 300 mg once daily. CrCl 30–50
(e.g., clarithromycin, ketoconazole, mL/min: 400 mg once daily. Ph+CML
ritonavir, miSOPROStol, nafcillin, (newly diagnosed): CrCl less than 30
salmeterol), moderate CYP3A4 in- mL/min: 200 mg once daily. CrCl 30–
hibitors (e.g., ciprofloxacin, diltia- 50 mL/min: 300 mg once daily.
ZEM, erythromycin, verapamil) may
CML with Baseline Hepatic Impairment
increase concentration/effect. Strong
PO: ADULTS: 200 mg once daily with food.
CYP3A4 inducers (e.g., rifAMPin,

Canadian trade name Non-Crushable Drug High Alert drug


148 brentuximab ­vedotin
Dosage Modification changes in serum electrolytes, LFT dur-
B Hepatotoxicity: Withhold treatment ing treatment. Offer antiemetics for nau-
until serum ALT, AST less than or equal to sea, vomiting. Monitor daily pattern of
2.5 times ULN. Then, resume at 400 mg bowel activity, stool consistency. Monitor
once daily with food. Discontinue if recov- CBC for neutropenia, thrombocytopenia,
ery lasts longer than 4 wks or hepatotox- anemia. Assess for bruising, hematuria,
icity, including elevated serum bilirubin jaundice, right upper abdominal pain,
levels greater than 2 times ULN. Severe weight loss, or acute infection (fever,
diarrhea: Withhold until recovery to diaphoresis, lethargy, productive cough).
low-grade diarrhea. Then, resume at 400
mg once daily with food. Myelosuppres- PATIENT/FAMILY TEACHING
sion: Withhold until absolute neutrophil • Blood levels will be drawn rou-
count greater than 1,000 cells/mm3 and tinely. • Take with meals. • Drink plenty
platelet count greater than 50,000 cells/ of fluids (diarrhea may result in dehydra-
mm3. Then, resume at same dose if recov- tion). • Swallow whole; do not break,
ery occurs within 2 wks. May reduce dose chew, crush, dissolve, or divide tab-
to 400 mg for recovery lasting greater than lets. • Strictly avoid pregnancy. •
2 wks. Use contraception during treatment and for
at least 30 days after treatment. • Report
SIDE EFFECTS urine changes, bloody or clay-colored stools,
Frequent (82%–35%): Diarrhea, nau- upper abdominal pain, nausea, vomiting,
sea, vomiting, abdominal pain, rash. bruising, persistent diarrhea, fever, cough,
Occasional (26%–10%): Pyrexia, fatigue, difficulty breathing, chest pain. • Immedi-
headache, cough, peripheral edema, ately report any newly prescribed medica-
arthralgia, anorexia, upper respiratory tions. • Avoid alcohol, grapefruit prod-
infection, asthenia, back pain, nasophar- ucts. • Discuss using antacids for
yngitis, dizziness, pruritus. indigestion, heartburn, upset stomach
(omeprazole, lansoprazole, pantoprazole
ADVERSE EFFECTS/TOXIC may reduce absorption, concentration of
REACTIONS bosutinib). • Separate antacid dosing by
Severe fluid retention may result in more than 2 hrs before and after medication.
pleural effusion, pericardial effusion,
pulmonary edema, ascites. Neutropenia,
thrombocytopenia, anemia is an ex-
pected response of drug therapy. Severe brentuximab ­vedotin
diarrhea may result in fluid loss, electro-
lyte imbalance, hypotension. Hepatotox- bren-tux-i-mab ve-doe-tin
icity occurred in 7%–9% of pts. (Adcetris)
j BLACK BOX ALERT jJC virus
NURSING CONSIDERATIONS infection resulting in progressive
multifocal leukoencephalopathy
BASELINE ASSESSMENT and death can occur.
Offer emotional support. Assess base- uCLASSIFICATION
line weight, BMP, LFT. Confirm negative
pregnancy test before initiating treatment. PHARMACOTHERAPEUTIC: Mono-
Obtain full medication history, including vi- clonal antibody, anti-CD30. CLINI-
tamins, herbal products. Screen for periph- CAL: Antineoplastic.
eral edema, signs/symptoms of HF, anemia.
INTERVENTION/EVALUATION
USES
Weigh daily and monitor for unexpected Treatment of relapsed or refractory clas-
rapid weight gain, edema. Monitor for sical Hodgkin’s lymphoma after failure
underlined – top prescribed drug
brentuximab ­vedotin 149
of autologous hematopoietic stem cell ketoconazole) increase concentra-
transplant (HSCT) or after failure of at tion/effect. CYP3A4 inducers (e.g., B
least two prior multiagent chemotherapy rifAMPin) may reduce concentration/
regimens or in pts who are not transplant effect. May decrease therapeutic effect of
candidates. Treatment of classical Hodg- BCG (intravesical), vaccines (live).
kin’s lymphoma, previously untreated May increase adverse effects of belim-
stage III or IV. Treatment of classical umab, bleomycin, natalizumab, vac-
Hodgkin’s lymphoma in pts at high risk of cines (live). HERBAL: Echinacea may
relapse or progression as post autologous decrease effect. FOOD: None known.
HSCT consolidation. Treatment of systemic LAB VALUES: May decrease Hgb, Hct,
anaplastic large-cell lymphoma (ALCL) af- WBC, RBC, platelets. May increase serum
ter failure of at least one prior multiagent bicarbonate, lactate dehydrogenase, glu-
chemotherapy regimen. Treatment of pre- cose, albumin, magnesium, sodium.
viously untreated systemic ALCL, periph-
eral T-cell lymphoma (CD30-expressing) AVAILABILITY (Rx)
in combination with cyclophosphamide, Injection, Powder for Reconstitution: 50-
DOXOrubicin, and predniSONE. Treatment mg single-use vial.
of primary cutaneous ALCL in pts receiv-
ing prior systemic therapy. Treatment of ADMINISTRATION/HANDLING
CD30-expressing mycosis fungoides. IV

PRECAUTIONS Reconstitution • Reconstitute each 50-


Contraindications: Hypersensitivity to mg vial with 10.5 mL Sterile Water for In-
brentuximab. Avoid use with bleomycin jection, directing the stream toward wall of
(increased risk for pulmonary toxicity). vial and not at powder. • Gently swirl (do
Cautions: Renal/hepatic impairment, pe- not shake). • This will yield a concentra-
ripheral neuropathy, infusion reactions, tion of 5 mg/mL. • The dose for pts
neutropenia, tumor lysis syndrome, Ste- weighing over 100 kg should be calculated
vens-Johnson syndrome, pregnancy. for 100 kg. • Reconstituted solution must
be transferred to infusion bag with a mini-
ACTION mum 100 mL diluent, yielding a final con-
Binds to CD30-expressing cells, allowing centration of 0.4–1.8 mg/mL brentux-
the antibody to direct the drug to a target on imab. • Gently invert bag to mix solution.
lymphoma cells, disrupting the microtubule Rate of administration • Infuse over
network within the cell. Therapeutic Ef- 30 min.
fect: Induces cell cycle arrest, cell death. Storage • Discard if solution contains
particulate or is discolored; solution
PHARMACOKINETICS should appear clear to slightly opales-
Minimally metabolized. Protein binding: cent, colorless. • May store solution at
68%–82%. Excreted primarily in feces 36°–46°F. • Use within 24 hrs after
(72%). Half-life: 4–6 days. reconstitution.

LIFESPAN CONSIDERATIONS IV COMPATIBILITIES


Pregnancy/Lactation: May cause fetal 0.9% NaCl, D5W, lactated Ringer’s.
harm (embryo-fetal toxicities). Unknown INDICATIONS/ROUTES/
if distributed in breast milk. Children/ El- DOSAGE
derly: Safety and efficacy not established.
b ALERT c Do not give by IV bolus or
INTERACTIONS IV push.
DRUG: Strong CYP3A4 inhibitors
(e.g., atazanavir, clarithromycin,

Canadian trade name Non-Crushable Drug High Alert drug


150 brentuximab ­vedotin
Hodgkin’s Lymphoma (Relapsed or Dosage in Renal Impairment
B Refractory) CrCl less than 30 mL/min: Avoid use.
IV infusion: ADULTS, ELDERLY: 1.8 mg/
kg (Maximum: 180 mg) infused over 30 Dosage in Hepatic Impairment
min q3wks. Continue treatment until dis- Mild impairment: Initial dose1.2 mg/
ease progression or unacceptable toxicity. kg (Maximum: 120 mg) q3wks. Moder-
ate to severe impairment: Avoid use.
Hodgkin’s Lymphoma (After HSCT)
IV infusion: ADULTS/ELDERLY: 1.8 mg/ SIDE EFFECTS
kg (Maximum: 180 mg) infused over b ALERT c Effects present as mild,
30 min every 3 wks. Continue treatment manageable.
until a maximum of 16 cycles, disease Frequent (52%–22%): Peripheral neurop-
progression, or unacceptable toxicity oc- athy, fatigue, respiratory tract infection,
curs. Begin within 4–6 wks post HSCT or nausea, diarrhea, fever, rash, abdomi-
upon recovery from HSCT. nal pain, cough, vomiting. Occasional
Hodgkin’s Lymphoma (Previously (19%–11%): Headache, dizziness, consti-
Untreated) pation, chills, bone/muscle pain, insom-
IV infusion: ADULTS, ELDERLY: 1.2 mg/ nia, peripheral edema, alopecia. Rare
kg (Maximum: 120 mg) q2wks (in (10%–5%): Anxiety, muscle spasm, de-
combination with doxorubicin, vinblas- creased appetite, dry skin.
tine, and dacarbazine [AVD]). Begin ADVERSE EFFECTS/TOXIC
within 1 hr after completion of AVD until REACTIONS
a maximum of 12 doses, disease progres-
sion, or unacceptable toxicity occurs. Myelosuppression characterized as neu-
tropenia (54% of pts), peripheral neu-
Mycosis Fungoides ropathy (52% of pts), thrombocytopenia
IV infusion: ADULTS, ELDERLY: 1.8 mg/kg (28% of pts), anemia (19% of pts) have
(Maximum: 180 mg) q3wks. Continue occurred. Infusion reactions (includ-
until a maximum of 16 cycles, disease ing anaphylaxis), Stevens-Johnson syn-
progression, or unacceptable toxicity. drome have been reported. Tumor lysis
Systemic Anaplastic Large-Cell
syndrome may lead to acute renal failure.
Lymphoma (ALCL) (Relapsed)
Progressive multifocal leukoencephalop-
IV infusion: ADULTS/ELDERLY: 1.8 mg/ athy (changes in mood, confusion, loss of
kg (Maximum: 180 mg) infused over memory, decreased strength or weakness
30 min q3wks. Continue treatment until on one side of body, changes in speech,
disease progression or unacceptable tox- walking, and vision) has been reported.
icity occurs. NURSING CONSIDERATIONS
Systemic ALCL, Peripheral T-Cell BASELINE ASSESSMENT
Lymphoma (CD30-Expressing) Obtain baseline CBC before treatment be-
(Previously Untreated) gins and as needed to monitor response
IV infusion: ADULTS/ELDERLY: 1.8 mg/ and toxicity but particularly prior to each
kg Maximum: 180 mg) q3wks for 6–8 dosing cycle. Question for evidence of
doses (in combination with cyclophospha- peripheral neuropathy (hypoesthesia, hy-
mide, DOXOrubicin, and predniSONE). peresthesia, paresthesia, burning sensa-
Primary Cutaneous ALCL (Relapsed)
tion, neuropathic pain or weakness). Pts
IV infusion: ADULTS/ELDERLY: 1.8
mg/ experiencing new or worsening neuropa-
kg (Maximum: 180 mg) q3wks for up thy may require a delay, dose change, or
to 16 cycles. discontinuation of treatment.

underlined – top prescribed drug


brexpiprazole 151
INTERVENTION/EVALUATION USES
Offer antiemetics to control nausea, Adjunctive therapy to antidepressants for B
vomiting. Monitor for hematologic tox- the treatment of major depressive dis-
icity (fever, sore throat, signs of local order. Treatment of schizophrenia. OFF-
infection, bruising, unusual bleeding), LABEL: Psychosis/agitation associated
symptoms of anemia (excessive fatigue, with dementia.
weakness). Assess response to medica-
tion. Monitor and report nausea, vomit- PRECAUTIONS
ing, diarrhea. Monitor daily pattern of Contraindications: Hypersensitivity to
bowel activity, stool consistency. Assess br­expiprazole. Cautions: Concurrent use
skin for evidence of rash. of CNS depressants (including alcohol)
PATIENT/FAMILY TEACHING antihypertensives, disorders in which
CNS depression is a feature, cardiovascu-
• Avoid crowds, persons with known lar or cerebrovascular disease (may in-
infections. • Report signs of infection duce hypotension), Parkinson’s disease,
at once (fever, flu-like symp- Parkinson’s disease dementia, Lewy body
toms). • Avoid contact with those who dementia, history of seizures or condi-
recently received live virus vac- tions that may lower seizure threshold
cine. • Do not receive immunizations (Alzheimer’s disease). Pts at risk for as-
without physician’s approval (drug low- piration pneumonia, elderly, HF, diabetes.
ers body resistance). • Promptly report Pts at high risk for suicide. Preexisting
fever, easy bruising, or unusual bleeding low WBC/ANC, history of drug-induced
from any site. • Male pts should be leukopenia/neutropenia, dehydration.
warned of potential risk to their repro-
ductive capacities. ACTION
Exact mechanism of action unknown. Pro-
vides partial agonist activity at DOPamine
and serotonin (5-HT1A) receptors and
brexpiprazole antagonist activity at serotonin (5-HT2A)
receptors. Therapeutic Effect: Dimin-
brex-pip-ra-zole ishes schizophrenic, depressive behavior.
(Rexulti)
j BLACK BOX ALERT jElderly pts PHARMACOKINETICS
with dementia-related psychosis
are at increased risk of death, Widely distributed. Metabolized in liver.
mainly due to HF, pneumonia. Protein binding: greater than 99%. Peak
Increased risk of suicidal thoughts plasma concentration: 4 hrs. Steady state
and behaviors in patients aged 24 reached in 10–12 days. Excreted in urine
yrs and younger with major depres- (25%), feces (46%). Half-life: 86–91
sion, other psychiatric disorders.
hrs.
Do not confuse brexpiprazole
with ARIPiprazole, esomepra- LIFESPAN CONSIDERATIONS
zole, omeprazole, or pantopra- Pregnancy/Lactation: Unknown if
zole, or RABEprazole. distributed in breast milk. May cause
uCLASSIFICATION extrapyramidal and/or withdrawal symp-
toms in neonates if given in third trimes-
PHARMACOTHERAPEUTIC: DOPa-
ter. Children: Safety and efficacy not
mine agonist. CLINICAL: Second- established. Elderly: May have in-
generation (atypical) antipsychotic creased risk for adverse effects due to
agent. age-related hepatic, renal, cardiac dis-
ease. May increase risk of death in elderly
pts with dementia-related psychosis.
Canadian trade name Non-Crushable Drug High Alert drug
152 brexpiprazole
CYP2D6 poor metabolizers or pts
INTERACTIONS
B taking strong CYP2D6 inhibitors or
DRUG: Alcohol may potentiate cognitive strong CYP3A4 inhibitors: Adminis-
and motor effects. Strong CYP3A4 induc- ter half of the usual dose. CYP2D6 poor
ers (e.g., carBAMazepine, rifAMPin) metabolizers taking strong/moder-
may decrease concentration/effect. Strong ate CYP3A4 inhibitors or pts taking
CYP3A4 inhibitors (e.g., itraconazole, strong/moderate CYP2D6 inhibi-
ketoconazole), strong CYP2D6 inhibi- tors with strong/moderate CYP3A4
tors (e.g., FLUoxetine, PARoxetine) inhibitors: Administer a quarter of
may increase concentration/effect. Meto- the usual dose. Pts taking strong
clopramide may increase adverse effects. CYP3A4 inducers: Double the usual
HERBAL: St John’s wort may decrease dose over 1–2 wks.
concentration. Gotu kola, kava kava,
valerian may increase CNS depression. SIDE EFFECTS
FOOD: None known. LAB VALUES: May Occasional (9%–4%): Headache, nasophar-
decrease leukocytes, neutrophils. May in- yngitis, dyspepsia, akathisia, somnolence,
crease serum blood glucose, lipid levels. tremor. Rare (3%–1%): Constipation, fa-
tigue, increased appetite, weight gain, anxi-
AVAILABILITY (Rx) ety, restlessness, dizziness, diarrhea, blurry
Tablets:0.25 mg, 0.5 mg, 1 mg, 2 mg, vision, dry mouth, salivary hypersecretion,
3 mg, 4 mg. abdominal pain, flatulence, myalgia, abnor-
mal dreams, insomnia, hyperhidrosis.
ADMINISTRATION/HANDLING
PO ADVERSE EFFECTS/TOXIC
REACTIONS
• Give without regard to food.
May increase risk of death in elderly pts
INDICATIONS/ROUTES/DOSAGE with dementia-related psychosis. Most
deaths appeared to be cardiovascular
Major Depressive Disorder (MDD)
(e.g., HF, sudden death) or infectious
PO: ADULTS, ELDERLY: Initially, 0.5–1 mg
(e.g., pneumonia) in nature. Increased in-
once daily. May increase at weekly inter-
cidence of suicidal thoughts and behaviors
vals up to 1 mg (if initial dose is 0.5 mg)
in pts 24 yrs and younger was reported.
once daily, then up to target dose of 2 mg
May increase risk of neuroleptic malignant
once daily. Maximum: 3 mg once daily.
syndrome (NMS). Symptoms of NMS may
Schizophrenia include hyperpyrexia, muscle rigidity, al-
PO: ADULTS, ELDERLY: Initially, 1 mg tered mental status, autonomic instability
once daily on days 1–4. May increase to (irregular pulse or blood pressure, tachy-
2 mg once daily on days 5–7, then to 4 cardia, diaphoresis, and cardiac dysrhyth-
mg once daily on day 8 based on clinical mia), elevated creatinine, phosphokinase,
response and tolerability. Maximum: 4 myoglobinuria (rhabdomyolysis), acute
mg once daily. renal failure. Metabolic changes such as
hyperglycemia, ketoacidosis, hyperosmo-
Dosage in Renal Impairment lar coma, diabetes, dyslipidemia, dystonia,
CrCl less than 60 mL/min: Maxi- and weight gain may occur. Other adverse
mum: 2 mg once daily for MDD, or 3 effects may include leukopenia, neutro-
mg once daily for schizophrenia. penia, agranulocytosis, orthostatic hypo-
tension, syncope, cerebrovascular events
Dosage in Hepatic Impairment (e.g., CVA, transient ischemic attack), sei-
Maximum: 2 mgonce daily for MDD, or zures, hyperthermia, dysphagia, cognitive
3 mg once daily for schizophrenia. or motor impairment, tardive dyskinesia.

underlined – top prescribed drug


brigatinib 153

NURSING CONSIDERATIONS uCLASSIFICATION


PHARMACOTHERAPEUTIC: Anaplas- B
BASELINE ASSESSMENT tic lymphoma tyrosine kinase inhibi-
Obtain baseline BMP, capillary blood glu- tor. CLINICAL: Antineoplastic.
cose, vital signs; CBC in pts with preex-
isting low WBC or history of leukopenia
or neutropenia. Receive full medication USES
history and screen for drug interactions. Treatment of pts with anaplastic lymphoma
Assess behavior, appearance, emotional kinase (ALK)–positive metastatic non–
state, response to environment, speech small-cell lung cancer (NSCLC) who have
pattern, thought content. Correct dehy- progressed or are intolerant to crizotinib.
dration, hypovolemia. Assess for suicidal
tendencies, history of dementia-related PRECAUTIONS
psychosis, HF, CVA, NMS, diabetes. Contraindications: Hypersensitivity to
INTERVENTION/EVALUATION
brigatinib. Cautions: Baseline anemia,
leukopenia. History of symptomatic bra-
Monitor weight, BMP, capillary blood dycardia, bradyarrhythmias, diabetes,
glucose, vital signs. Diligently monitor for hepatic/renal impairment, hypertension,
extrapyramidal symptoms, tardive dys- ocular disease, pancreatitis, pulmo-
kinesia, hypotension, syncope, cerebro- nary disease. Concomitant use of strong
vascular or cardiovascular dysfunction, CYP3A inhibitors, beta blockers, calcium
NMS. Assess for therapeutic response channel blockers (see Interactions).
(greater interest in surroundings, im-
proved self-care, increased ability to con- ACTION
centrate, relaxed facial expression). A broad-spectrum kinase inhibitor (ac-
PATIENT/FAMILY TEACHING tivity against EGFR, ALK, ROSI, IGF-1R
• Avoid alcohol. • Avoid tasks that re- and FLT-3). Inhibits ALK downstream
quire alertness, motor skills until response signaling proteins. Has activity against
to drug is established. • Report worsening cells expressing EML4-ALK. Therapeu-
depression, suicidal ideation, abnormal tic Effect: Expresses anti-tumor activity
changes in behavior. • Treatment may against EML-ALK mutant forms shown in
cause life-threatening conditions such as NSCLC in pts progressed with crizotinib.
involuntary, uncontrollable movements, el- PHARMACOKINETICS
evated body temperature, altered mental
status, high or low blood pressure, sei- Widely distributed. Metabolized in liver.
zures. • Pts with HF or active pneumonia Protein binding: 66%. Peak plasma con-
are at increased risk of sudden centration: 1–4 hrs. Excreted in feces
death. • Immediately report fever, cough, (65%), urine (25%). Half-life: 25 hrs.
increased sputum production, palpitations, LIFESPAN CONSIDERATIONS
fainting, or signs of HF.
Pregnancy/Lactation: Avoid preg-
nancy; may cause fetal harm. Females of
reproductive potential should use effective
brigatinib nonhormonal contraception during treat-
ment and for at least 4 mos after discon-
bri-ga-ti-nib tinuation. Unknown if distributed in breast
(Alunbrig) milk. Breastfeeding not recommended
Do not confuse brigatinib with during treatment and for at least 1 wk
axitinib, cabozantinib, ceritinib, after discontinuation. Males: Males with
crizotinib, erlotinib, imatinib. female partners of reproductive potential

Canadian trade name Non-Crushable Drug High Alert drug


154 brigatinib
should use barrier methods during sexual daily for 7 days before increasing to the
B activity during treatment for at least 3 mos dose that was previously tolerated.
after discontinuation. Children: Safety
Dose Reduction Schedule
and efficacy not established. Elderly: No
First dose reduction: 90 MG ONCE
age-related precautions noted.
DAILY: Reduce to 60 mg once daily. 180 MG
INTERACTIONS ONCE DAILY: Reduce to 120 mg once daily.
Second dose reduction: 90 MG ONCE
DRUG: Strong CYP3A4 inhibitors
DAILY: Permanently discontinue. 180 MG
(e.g., clarithromycin, itraconazole,
ONCE DAILY: Reduce to 90 mg once daily.
ritonavir) may increase concentra-
Third dose reduction: 90 MG ONCE
tion/effect. Strong CYP3A4 inducers
DAILY: N/A. 180 MG ONCE DAILY: Reduce
(e.g., carbamazepine, phenytoin,
rifampin) may decrease concentra- to 60 mg once daily. Note: Once dose
tion/effect. May decrease effectiveness of has been reduced, do not subsequently
hormonal contraceptives. Concomitant increase dose. If pt is unable to tolerate
use of beta blockers (e.g., atenolol, 60-mg dose, permanently discontinue.
carvedilol, metoprolol), calcium Dose Modification
channel blockers (e.g., diltiazem, Symptomatic Bradycardia
verapamil), digoxin may increase Withhold treatment until recovery to as-
risk of symptomatic bradycardia. ymptomatic bradycardia or to a heart
HERBAL: St. John’s wort may decrease rate of 60 bpm or greater, then resume
concentration/effect. FOOD: Grapefruit at ­reduced dose level (if pt not taking
products may increase concentration/ concomitant medications known to cause
effect. LAB VALUES: May increase serum bradycardia). Symptomatic bradycar-
alkaline phosphatase, ALT, AST, amylase, dia in pts taking concomitant medi-
bilirubin, CPK, glucose, lipase. May de- cations known to cause bradycar-
crease Hct, Hgb, lymphocytes, RBCs; se- dia: Withhold treatment until recovery to
rum phosphate. May prolong aPTT. asymptomatic bradycardia or heart rate of
AVAILABILITY (Rx) 60 bpm or greater. If concomitant medi-
cation can be adjusted or discontinued,
Tablets: 30 mg, 90 mg, 180 mg. then resume at same dose. If concomitant
medication cannot be adjusted or discon-
ADMINISTRATION/HANDLING tinued, then resume at reduced dose level.
PO Life-threatening bradycardia in pts
• Give with or without food. • Admin- who are not taking concomitant
ister tablets whole; do not break, crush, medications known to cause brady-
cut, or divide. • If a dose is missed or cardia: Permanently discontinue. Life-
vomiting occurs after administration, do threatening bradycardia in pts who
not give extra dose. Administer next dose are taking concomitant medications
at regularly scheduled time. known to cause bradycardia: With-
hold treatment until recovery to asymptom-
INDICATIONS/ROUTES/DOSAGE atic bradycardia or heart rate of 60 bpm or
Non–Small-Cell Lung Cancer (Metastatic, greater. If concomitant medication can be
ALK-Positive) adjusted or discontinued, then resume at
PO: ADULTS, ELDERLY: 90 mg once daily reduced dose level with frequent monitor-
for 7 days. If 90-mg dose is tolerated, then ing. Permanently discontinue if symptomatic
increase to 180 mg once daily. Continue bradycardia recurs despite dose reduction.
until disease progression or unacceptable CPK Elevation
toxicity. Note: If treatment is interrupted CTCAE Grade 3 CPK elevation
for 14 days (or more) for reasons other (greater than 5 times upper limit of
than toxic reactions, restart at 90 mg once normal [ULN]): Withhold treatment until
underlined – top prescribed drug
brigatinib 155
recovery to baseline or less than or equal Pulmonary
to 2.5 times ULN, then resume at same CTCAE Grade 1 pulmonary symp- B
dose. CTCAE Grade 4 CPK elevation toms during the first 7 days of ther-
(greater than 10 times ULN) or recur- apy: Withhold treatment until recovery to
rence of CTCAE Grade 3 CPK eleva- baseline, then resume at same dose level.
tion: Withhold treatment until recovery to Do not increase dose if interstitial lung dis-
baseline or less than or equal to 2.5 times ease (ILD)/pneumonitis suspected. CTCAE
ULN, then resume at reduced dose level. Grade 1 pulmonary symptoms after
the first 7 days of therapy: Withhold
Hyperglycemia treatment until recovery to baseline, then
CTCAE Grade 3 serum glucose el- resume at same dose level. CTCAE Grade
evation (greater than 250 mg/dL 2 pulmonary symptoms during the
or 13.9 mmol/L): If adequate medical first 7 days of therapy: Withhold treat-
management of hyperglycemia cannot ment until recovery to baseline, then re-
be achieved, withhold treatment until sume at reduced dose level. Do not increase
adequately controlled. Consider dose dose if ILD/pneumonitis suspected. CTCAE
reduction or permanent discontinuation. Grade 2 pulmonary symptoms after
the first 7 days of therapy: Withhold
Hypertension
CTCAE Grade 3 hypertension (sys-
treatment until recovery to baseline, then
tolic B/P greater than or equal to
resume at same dose level. If ILD/pneumo-
160 mm Hg or diastolic B/P greater
nitis is suspected, resume at reduced dose
than or equal to 100 mm Hg); con-
level. With any recurrence of ILD/pneumo-
comitant use of more than one
nitis or any Grade 3 or 4 pulmonary symp-
antihypertensive drug; required
toms, permanently discontinue.
medical intervention; requirement Visual Disturbance
of aggressive hypertensive ther- CTCAE Grade 2 or 3 visual distur-
apy: Withhold treatment until recovery bance: Withhold treatment until recovery
to Grade 1 or 0, then resume at reduced to baseline, then resume at reduced dose
dose level. CTCAE Grade 4 hyperten- level. Grade 4 visual disturbance: Per-
sion (first occurrence) or recurrence manently discontinue.
of Grade 3 hypertension: Withhold
treatment until recovery to Grade 1 or Other Toxicities
0, then either resume at reduced dose Any other CTCAE Grade 3 toxic-
level or permanently discontinue. Recur- ity: Withhold treatment until recovery to
rence of Grade 4 hypertension: Per- baseline, then resume at same dose level.
manently discontinue. Recurrence of any other Grade 3 tox-
icity: Withhold treatment until recovery
Lipase/Amylase Elevation to baseline, then either resume at reduced
CTCAE Grade 3 serum amylase or li- dose level or permanently discontinue.
pase elevation (greater than 2 times First occurrence of any other CTCAE
upper limit of normal [ULN]): With- Grade 4 toxicity: Withhold treatment
hold treatment until recovery to Grade until recovery to baseline, then either re-
1 or 0 (or baseline), then resume at sume at reduced dose level or permanently
same dose. CTCAE Grade 4 serum discontinue. Recurrence of any other
amylase or lipase elevation (greater Grade 4 toxicity: Permanently discon-
than 5 times ULN) or recurrence of tinue. Concomitant use of strong
Grade 3 serum lipase or amylase CYP3A inhibitors: Reduce daily dose
elevation: Withhold treatment until by 50% if strong CYP3A inhibitor cannot
recovery to Grade 1 or 0, then resume at be discontinued. If strong CYP3A inhibi-
reduced dose level. tor is discontinued, then resume the dose

Canadian trade name Non-Crushable Drug High Alert drug


156 brigatinib
that was previously tolerated before start- prior to initiation. Obtain nutritional con-
B ing CYP3A inhibitor. sult. Offer emotional support.
Dosage in Renal Impairment INTERVENTION/EVALUATION
Mild to moderate impairment: No dose Monitor CBC, CPK, BMP, LFT; vital signs
adjustment. Severe impairment: Not (esp. heart rate) periodically. Obtain
specified; use caution. serum amylase, lipase in pts with severe
Dosage in Hepatic Impairment abdominal pain, nausea, periumbilical
Mild impairment: No dose adjustment. ecchymosis (Cullen’s sign), flank ec-
Moderate to severe impairment: Not chymosis (Grey Turner’s sign). Monitor
specified; use caution. for hepatotoxicity, hyperglycemia, vision
changes, myalgia, musculoskeletal pain,
SIDE EFFECTS interstitial lung disease/pneumonitis. If
Frequent (33%–19%): Nausea, fatigue, treatment-related toxicities occur, con-
headache, dyspnea, vomiting, decreased sider referral to specialist; pt may require
appetite, diarrhea, constipation. Oc- treatment with corticosteroids. Screen for
casional (18%–9%): Cough, abdominal acute infections. Monitor I&O, hydration
pain, rash (acneiform dermatitis, exfo- status, stool frequency and consistency.
liative rash, pruritic rash, pustular rash), Encourage proper calorie intake and nu-
pyrexia, arthralgia, peripheral neuropa- trition. Assess skin for rash, lesions.
thy, muscle spasm, extremity pain, hyper- PATIENT/FAMILY TEACHING
tension, back pain, myalgia.
• Treatment may depress your immune
ADVERSE EFFECTS/TOXIC system and reduce your ability to fight in-
REACTIONS fection. Report symptoms of infection,
Anemia, leukopenia are expected re- such as body aches, burning with urina-
sponses to therapy. Serious events, such tion, chills, cough, fatigue, fever. Avoid
as ILD/pneumonitis (3%–9% of pts), hy- those with active infection. • Therapy
pertension (6%–21% of pts), symptom- may decrease your heart rate, which may
atic bradycardia (6%–7% of pts), visual be life-threatening; report dizziness, chest
disturbance (blurred vision, diplopia, re- pain, palpitations, or fainting. • Worsen-
duced visual acuity, macular edema, vit- ing cough, fever, or shortness of breath
reous floaters, visual field defect, vitreous may indicate severe lung inflamma-
detachment, cataract [7%–10% of pts]), tion. • Avoid pregnancy. Do not breast-
CPK elevation (27%–48% of pts), pan- feed. Females of childbearing potential
creatic enzyme elevation (27%–39%), should use effective contraception during
hyperglycemia (43% of pts), may occur. treatment and up to 4 mos after final dose.
Males with female partners of reproduc-
NURSING CONSIDERATIONS tive potential should use condoms during
sexual activity during treatment and for up
BASELINE ASSESSMENT to 3 mos after final dose. • Blurry vision,
Obtain baseline CBC, CPK, BMP, LFT; urine confusion, frequent urination, increased
pregnancy, vital signs. Obtain baseline ECG thirst, fruity breath may indicate high
in pts with history of arrhythmia, HF. Ques- blood sugar levels. • Report abdominal
tion plans for breastfeeding. Question his- pain, bruising around belly button or flank
tory of hepatic/renal impairment, diabetes, bruising, black/tarry stools, dark-colored
cardiac/pulmonary disease, hypertension, urine, decreased urine output, severe
pancreatitis. Receive full medication his- muscle aches, yellowing of the skin or
tory and screen for interactions. Assess eyes. • Do not take newly prescribed
visual acuity. Verify ALK-positive NSCLC test medication unless approved by the d­ octor

underlined – top prescribed drug


brivaracetam 157
who originally started treatment. • Do breastfeeding. Children: Safety and
not ingest grapefruit products. efficacy not established in pts younger B
than 16 yrs. Elderly: Not specified;
use caution.
INTERACTIONS
brivaracetam DRUG: RifAMPin may decrease concen-
tration/effect. May increase concentration/
briv-a-ra-se-tam effect of carBAMazepine. CNS depres-
(Briviact, Brivlera ) sants (e.g., alcohol, morphine, oxy-
Do not confuse brivaracetam CODONE, zolpidem) may increase CNS
with levETIRAcetam. depressant effect. HERBAL: Herbals with
uCLASSIFICATION sedative properties (e.g., chamomile,
kava kava, valerian) may increase
PHARMACOTHERAPEUTIC: Synap- CNS depression. FOOD: None known.
tic vesicle protein 2A ligand. CLINI- LAB VALUES: May decrease neutrophils,
CAL: Anticonvulsant, miscellaneous.
WBCs. May increase serum phenytoin
(free and total) levels.
USES
AVAILABILITY (Rx)
Monotherapy or adjunctive therapy in the
Tablets: 10 mg, 25 mg, 50 mg, 75 mg,
treatment of partial-onset seizures in pts
100 mg. Oral Solution: 10 mg/mL. Injec-
4 years and older with epilepsy.
tion Solution: 50 mg/5 mL.
PRECAUTIONS
ADMINISTRATION/HANDLING
Contraindications: Hypersensitivity to
brivaracetam. Cautions: Baseline neu- IV
tropenia, hepatic impairment; pts at high Reconstitution • Visually inspect for
risk for suicide; history of depression, particulate matter or discoloration. Do
mood disorder, psychiatric disorder; his- not use if particulate matter or discolor-
tory of drug abuse. ation observed. • May be given without
ACTION further dilution or may be mixed with
0.9% NaCl, 5% dextrose injection.
Exact mechanism unknown. Has high af- Rate of administration • Give over
finity for synaptic vesicle protein 2A in the 2–15 min.
brain. Therapeutic Effect: Prevents Storage • Injection solution should
seizure activity. appear clear and colorless. • Diluted
PHARMACOKINETICS solution should not be stored more than
4 hrs at room temperature. Do not
Rapidly, completely absorbed following freeze.
PO administration. Metabolized primar-
ily by enzymatic hydrolysis, mediated by PO
hepatic and extrahepatic amidase. Pro- • Give without regard to food. • Admin-
tein binding: less than or equal to 20%. ister tablets whole; do not crush, cut, dis-
Peak plasma concentration: 1 hr. Pri- solve, or divide. • Oral solution should
marily excreted in urine (95%). Half- appear slightly viscous, clear, colorless to
life: 9 hrs. yellowish in color, and have a raspberry
flavor. • Store oral solution at room
LIFESPAN CONSIDERATIONS temperature. • Discard unused oral so-
Pregnancy/Lactation: Unknown lution remaining after 5 mos of first open-
if distributed in breast milk. Must ei- ing bottle. • Do not freeze oral solution.
ther discontinue drug or discontinue Oral solution should be delivered using
Canadian trade name Non-Crushable Drug High Alert drug
158 brivaracetam
calibrated measuring device (does not normal coordination, nystagmus, irritability,
B require dilution). May give oral solution constipation.
via nasogastric tube or gastrostomy tube.
ADVERSE EFFECTS/TOXIC
INDICATIONS/ROUTES/DOSAGE REACTIONS
Partial-Onset Seizures (Monotherapy or Sudden discontinuance may increase risk
Adjunctive Therapy) of seizure frequency and status epilepti-
PO/IV: ADULTS, CHILDREN 16 YRS AND cus. May increase risk of suicidal thoughts
OLDER: Initially, 50 mg twice daily. May or behavior. Psychiatric events including
either decrease to 25 mg twice daily or nonpsychotic behavior (anger, agitation,
increase to 100 mg twice daily. Main- aggression, anxiety, apathy, depression,
tenance: 25–100 mg twice daily. hyperactivity, irritability, mood swings,
Maximum: 200 mg/day. When initiat- nervousness, restlessness, tearfulness)
ing treatment, gradual dose escalation is and psychotic symptoms (psychotic be-
not required. Injection solution should havior with acute psychosis, delirium,
be administered at same dose and same hallucinations, paranoia) occurred in
frequency as tablets and oral solution. 13% of pts. Hypersensitivity reactions in-
Gradually taper dose to discontinue treat- cluding bronchospasm, angioedema were
ment (50 mg/day on a weekly basis with reported. Clinically significant decreased
final week of treatment at dose of 20 WBC count (less than 3,000 cells/mm3)
mg/day). ELDERLY: Consider initiating at and decreased neutrophil count (less than
lower end of the dosage range. CHILDREN 1,000 cells/mm3) occurred in 1.8% and
4 TO 15 YRS WEIGHING 50 KG OR MORE: Ini- 0.3% of pts, respectively.
tially, 25–50 mg twice daily. May in-
crease up to maximum of 100 mg twice NURSING CONSIDERATIONS
daily. WEIGHING 20–49 KG: Initially, 0.5–1 BASELINE ASSESSMENT
mg/kg twice daily. May increase up to Obtain CBC in pts with baseline neutro-
maximum of 2 mg/kg twice daily. WEIGH- penia. Review history of seizure disorder
ING 11–19 KG: Initially, 0.5–1.25 mg/kg
(intensity, frequency, duration, LOC).
twice daily. May increase up to maximum Initiate seizure precautions, fall precau-
of 2.5 mg/kg twice daily. tions. Question history of hypersensitivity
Dose Modification reaction, hepatic impairment, psychiatric
Concomitant use with rifAMPin: May disorder; history of suicidal thoughts or
need to increase brivaracetam dosage by behavior. Obtain urine pregnancy in fe-
100% (double dose). male pts of reproductive potential.
INTERVENTION/EVALUATION
Dosage in Renal Impairment
No dosage adjustment. Not recom- Periodically monitor CBC in pts with neu-
mended in pts with ESRD undergoing tropenia. Monitor phenytoin levels in pts
dialysis (not studied). taking concomitant phenytoin (treatment
may increase phenytoin levels). Observe
Dosage in Hepatic Impairment for recurrence of seizure activity. Assess
Mild, moderate, severe impair- for clinical improvement (decrease in in-
ment: Initially, 25 mg twice daily. tensity/frequency of seizures). Diligently
Maintenance: 25–75 mg twice daily. monitor for depression, changes in be-
Maximum: 75 mg twice daily. havior, psychosis, suicidal ideation. Assist
with ambulation if dizziness occurs.
SIDE EFFECTS
Occasional (16%–9%): Somnolence, sed­ PATIENT/FAMILY TEACHING
ation, dizziness, fatigue. Rare (5%–2%): Nau- • Drowsiness usually diminishes with
sea, vomiting, ataxia, balance disorder, ab- continued therapy. • Avoid tasks that

underlined – top prescribed drug


brodalumab 159
require alertness, motor skills until re- tions: Baseline neutropenia; history of
sponse to drug is established. • Do not anxiety, depression, suicidal ideation and B
abruptly discontinue medication (may behavior, mood disorder; concomitant
precipitate seizures). • Strict mainte- immunosuppressant therapy, conditions
nance of drug therapy is essential for predisposing to infection (e.g., diabetes,
seizure control. • Report anxiety, an- immunocompromised pts, renal failure,
ger, depression, mood swings, hostile open wounds), prior exposure to tuber-
behavior, thoughts of suicide, unusual culosis. Concomitant use of live vaccines
changes in behavior. • Difficulty not recommended. Not recommended in
breathing, swelling of tongue or throat pts with active TB.
may indicate emergent allergic reac-
tion. • Avoid alcohol. ACTION
Selectively binds to the IL-17A receptor,
inhibiting the release of pro-inflammatory
cytokines (involved in the pathogenesis
brodalumab of immune-mediated diseases, includ-
ing plaque psoriasis). Therapeutic
broe-dal-ue-mab Effect: Blocks cytokine-induced re-
(Siliq) sponses.
j BLACK BOX ALERT jSuicidal
ideation and behavior, including PHARMACOKINETICS
completed suicides, were reported Widely distributed. Metabolism: not spec-
with brodalumab. Screen for history ified. Degraded into small peptides and
of depression, suicidal ideation.
Recommend mental health consul- amino acids via catabolic pathway. Peak
tation for pts with suicidal ideation plasma concentration: 3 days. Steady
and behavior. Pts must seek imme- state reached in 4 wks. Excretion not
diate medical attention if new-onset specified. Half-life: Not specified.
suicidal ideation, anxiety, depres-
sion, mood change occur. LIFESPAN CONSIDERATIONS
Do not confuse brodalumab
with avelumab, dupilumab, Pregnancy/Lactation: Unknown if
durvalumab, nivolumab, or distributed in breast milk. However, hu-
sarilumab. man immunoglobulin G (IgG) is present
in breast milk and is known to cross the
uCLASSIFICATION placenta. Children: Safety and efficacy
PHARMACOTHERAPEUTIC: Anti- not established. Elderly: No age-related
interleukin 17-receptor antibody. precautions noted.
Monoclonal antibody. CLINICAL: An- INTERACTIONS
ti-psoriasis agent.
DRUG: May decrease therapeutic ef-
fect of BCG (intravesical), vaccines
USES (live). May increase adverse effects of
Treatment of moderate to severe plaque belimumab, natalizumab, vaccines
psoriasis in adults who are candidates (live). HERBAL: Echinacea may de-
for systemic therapy or phototherapy crease therapeutic effect. FOOD: None
and have failed to respond or have lost known. LAB VALUES: May decrease
response to other systemic therapies. neutrophils.

PRECAUTIONS AVAILABILITY (Rx)


Hypersensitivity to
Contraindications: Injection Solution: 210 mg/1.5 mL in
brodalumab. Crohn’s disease. Cau- prefilled single-dose syringe.

Canadian trade name Non-Crushable Drug High Alert drug


160 brodalumab

ADMINISTRATION/HANDLING ADVERSE EFFECTS/TOXIC


B REACTIONS
SQ
Preparation • Remove prefilled sy- Suicidal ideation and behavior, including
ringe from refrigerator and allow solu- completed suicides, were reported. May
tion to warm to room temperature (ap- increase risk of tuberculosis. Infections
prox. 30 min) with needle cap such as bronchitis, influenza, nasophar-
intact. • Visually inspect for particulate yngitis, pharyngitis, upper respiratory
matter or discoloration. Solution should tract infection, tinea infections, UTI
appear clear, colorless to slightly yellow may occur. May cause exacerbation of
in color. Do not use if solution is cloudy, Crohn’s disease and ulcerative colitis.
discolored, or if visible particles are ob- Immunogenicity (auto-brodalumab anti-
served. bodies) occurred in 3% of pts.
Administration • Insert needle subcu-
taneously into upper arms, outer thigh, NURSING CONSIDERATIONS
or abdomen, and inject solution. • Do BASELINE ASSESSMENT
not inject into areas of active skin disease
or injury such as sunburns, skin rashes, Obtain CBC in pts with known history
inflammation, skin infections, or active of neutropenia. Screen for active infec-
psoriasis. • Do not administer IV tion. Pts should be evaluated for active
or intramuscularly. • Rotate injection tuberculosis and tested for latent infec-
sites. tion prior to initiating treatment and pe-
Storage • Refrigerate prefilled sy-
riodically during therapy. Induration of 5
ringes in original carton until time of mm or greater with tuberculin skin test
use. • May store at room temperature should be considered a positive test re-
for up to 14 days. Once warmed to room sult when assessing if treatment for latent
temperature, do not place back into re- tuberculosis is necessary. Verify pt has
frigerator. • Do not freeze or expose to not received live vaccines prior to initia-
heating sources. • Do not shake. • tion. Question history of Crohn’s disease,
Protect from light. ulcerative colitis, hypersensitivity reac-
tion; anxiety, depression, mood disorder,
INDICATIONS/ROUTES/DOSAGE suicidal ideation and behavior. Conduct
Plaque Psoriasis
dermatological exam; record character-
SQ: ADULTS, ELDERLY: Initially, 210 mg istics of psoriatic lesions. Assess pt’s will-
once at wks 0, 1, 2, followed by 210 mg ingness to self-inject medication.
once q2wks thereafter. INTERVENTION/EVALUATION
Permanent discontinuation: Con-
sider discontinuation in pts who have Diligently monitor for suicidal ideation
not achieved an adequate response after and behavior, new onset or worsening
12–16 wks. of anxiety, depression, mood disorder.
Consult mental health professional if
Dosage in Renal/Hepatic Impairment mood disorder suspected. Monitor for
Not specified; use caution. symptoms of tuberculosis, including
those who tested negative for latent tu-
SIDE EFFECTS berculosis infection prior to initiation.
Occasional (5%–4%): Arthralgia, head- Interrupt or discontinue treatment if se-
ache. Rare (3%–1%): Fatigue, diarrhea, rious infection, opportunistic infection,
oropharyngeal pain, nausea, myalgia, or sepsis occurs, and initiate appropri-
injection site reactions (bruising, ery- ate antimicrobial therapy. Monitor for
thema, hemorrhage, pain, pruritus), hypersensitivity reaction, symptoms of
conjunctivitis. inflammatory bowel disease. Assess skin
for improvement of lesions.
underlined – top prescribed drug
budesonide 161
PATIENT/FAMILY TEACHING older. Nebulization, oral inhalation:
• Seek immediate medical attention if Maintenance or prophylaxis therapy for B
thoughts of suicide, new onset or wors- asthma in pts 6 yrs and older (dry powder
ening of anxiety, depression, or changes inhaler) or 12 mos to 8 yrs (nebulization).
in mood occurs. • A healthcare pro- PO: Treatment of mild to moderate active
vider will show you how to properly Crohn’s disease. Maintenance of clinical
prepare and inject your medication. You remission of mild to moderate Crohn’s
must demonstrate correct preparation disease. Induction of remission in active,
and injection techniques before using mild to moderate ulcerative colitis. OFF-
medication at home. • Treatment may LABEL: PO: Treatment of eosinophilic
depress your immune system response esophagitis. Nebulization/inhala-
and reduce your ability to fight infection. tion: Acute exacerbation of COPD.
Report symptoms of infection, such as
body aches, chills, cough, fatigue, fever. PRECAUTIONS
Avoid those with active infection. • Do Contraindications: Hypersensitivity to
not receive live vaccines. • Expect fre- budesonide (nebulization/inhalation), pri-
quent tuberculosis screening. • Report mary treatment of status asthmaticus, acute
travel plans to possible endemic ar- episodes of asthma. Not for relief of acute
eas. • Treatment may cause worsening bronchospasms. Nasal: Use in children
of Crohn’s disease or cause inflammatory younger than 6 yrs of age. Cautions: Thy-
bowel disease. Report abdominal pain, roid disease, hepatic impairment, renal im-
diarrhea, weight loss. pairment, cardiovascular disease, diabetes,
glaucoma, cataracts, myasthenia gravis, pts
at risk for osteoporosis, seizures, GI dis-
ease, post acute MI, elderly.
budesonide ACTION
bue-des-oh-nide Inhibits accumulation of inflammatory cells;
(Entocort EC, Pulmicort Flexhaler, controls rate of protein synthesis; decreases
Pulmicort, Rhinocort Allergy, Uceris) migration of polymorphonuclear leuko-
Do not confuse budesonide with cytes (reverses capillary permeability and
Budeprion. lysosomal stabilization at cellular level).
Therapeutic Effect: Relieves symptoms
FIXED-COMBINATION(S) of allergic rhinitis, asthma, Crohn’s disease.
Symbicort: budesonide/formoterol
(bronchodilator): 80 mcg/4.5 mcg, PHARMACOKINETICS
160 mcg/4.5 mcg. Form Onset Peak Duration
Pulmicort 2–8 days 4–6 wks —
uCLASSIFICATION Respules
PHARMACOTHERAPEUTIC: Glu- Rhinocort 10 hrs 2 wks —
cocorticosteroid. CLINICAL: Anti- Aqua
inflammatory, antiallergy. Minimally absorbed from nasal tissue;
moderately absorbed from inhalation.
Protein binding: 88%. Primarily metabo-
USES lized in liver. Half-life: 2–3 hrs.
Nasal: (Rx): Management of seasonal or
perennial allergic rhinitis in adults and LIFESPAN CONSIDERATIONS
children 6 yrs and older. (OTC): Relief Pregnancy/Lactation: Unknown if
of hay fever, other upper respiratory al- drug crosses placenta or is distributed in
lergies in adults and children 6 yrs and breast milk. Children: Prolonged treat-

Canadian trade name Non-Crushable Drug High Alert drug


162 budesonide
ment or high dosages may decrease short- PO
B term growth rate, cortisol secretion. El- • May take with or without food. Swal-
derly: No age-related precautions noted. low whole. Do not break, crush, dissolve,
or divide capsule or tablet.
INTERACTIONS
DRUG: CYP3A4 inhibitors (e.g., clar­ INDICATIONS/ROUTES/DOSAGE
ithromycin, ketoconazole, ritonavir) Rhinitis
may increase concentration. May decrease Intranasal: (Rx): ADULTS, ELDERLY, CHIL-
effect of aldesleukin, BCG (intravesi- DREN 6 YRS AND OLDER: 1 spray (32 mcg)
cal). May increase adverse effects of na- in each nostril once daily. Maximum: 4
talizumab. HERBAL: Echinacea may sprays in each nostril once daily for
decrease effects. FOOD: Grapefruit prod- adults and children 12 yrs and older; 2
ucts may increase systemic exposure. LAB sprays in each nostril once daily for chil-
VALUES: May decrease serum potassium. dren 6–11 yrs.
Intranasal: (OTC): ADULTS, ELDERLY, CHIL-
AVAILABILITY (Rx) DREN 6 YRS AND OLDER: 2 sprays in each
Oral Inhalation Powder: (Pulmicort Flex- nostril once daily. May decrease to 1
haler): 90 mcg per inhalation; 180 mcg per spray in each nostril once daily.
inhalation. Inhalation Suspension for Nebuli-
zation: (Pulmicort): 0.25 mg/2 mL; 0.5 mg/2 Bronchial Asthma
mL; 1 mg/2 mL. Nasal Spray: (Rhinocort Al- Nebulization: CHILDREN 12 MOS–8
lergy, Rhinocort Aqua): 32 mcg/spray. YRS: (Previous therapy with bronchodi-
Capsules, Delayed-Release: (En- lators alone): 0.5 mg/day as single dose
tocort EC): 3 mg. Tablets, Extended- or 2 divided doses. Maximum: 0.5 mg/
Release: (Uceris): 9 mg. day. (Previous therapy with inhaled corti-
costeroids): 0.5 mg/day as single dose or
ADMINISTRATION/HANDLING 2 divided doses. Maximum: 1 mg/day.
Inhalation (Previous therapy of oral corticosteroids):
• Hold inhaler in upright position to load 1 mg/day as single dose in 2 divided
dose. Do not shake prior to use. Prime prior doses. Maximum: 1 mg/day.
to first use only. • Place mouthpiece be- Oral inhalation: (Pulmicort Flex-
tween lips and inhale forcefully and deeply. haler): ADULTS, ELDERLY: Initially, 360
Do not exhale through inhaler; do not use a mcg 2 times/day. Maximum: 720
spacer. • Rinsing mouth after each use mcg 2 times/day. CHILDREN, 6 YRS AND
decreases incidence of candidiasis. OLDER: 180 mcg 2 times/day. Maxi-
mum: 360 mcg 2 times/day.
Intranasal
Crohn’s Disease
• Instruct pt to clear nasal passages before
use. • Tilt pt’s head slightly for- PO (capsule): ADULTS, ELDERLY: 9 mg
ward. • Insert spray tip into nostril, point- once daily for up to 8 wks. Recurring epi-
ing toward nasal passages, away from nasal sodes may be treated with a repeat 8-wk
septum. • Spray into one nostril while pt course of treatment. Maintenance of re-
holds other nostril closed and concurrently mission: 6 mg once daily for up to 3 mos.
inspires through nostril to allow medication Ulcerative Colitis
as high into nasal passages as possible. PO (tablet): ADULTS, ELDERLY: 9 mg
once daily in morning for up to 8 wks.
Nebulization
• Shake well before use. • Administer Dosage in Renal/Hepatic Impairment
with mouthpiece or face mask. • Rinse No dose adjustment.
mouth following treatment.

underlined – top prescribed drug


bumetanide 163

SIDE EFFECTS USES


Frequent (greater than 3%): Nasal: Mild Management of edema associated with B
nasopharyngeal irritation, burning, sting- HF, renal disease, or hepatic disease.
ing, dryness; headache, cough. Inha-
lation: Flu-like symptoms, headache, PRECAUTIONS
pharyngitis. Occasional (3%–1%): Nasal: Contraindications: Hypersensitivity to
Dry mouth, dyspepsia, rebound conges- bumetanide. Anuria, hepatic coma,
tion, rhinorrhea, loss of taste. Inhala- severe electrolyte depletion (until con-
tion: Back pain, vomiting, altered taste, dition improves or is corrected). Cau-
voice changes, abdominal pain, nausea, tions: Severe hypersensitivity to sulfon-
dyspepsia. amides; hypotension.
ADVERSE EFFECTS/TOXIC ACTION
REACTIONS Enhances excretion of sodium, chloride,
Acute hypersensitivity reaction (urticaria, and, to lesser degree, potassium by direct
angioedema, severe bronchospasm) oc- action at ascending limb of loop of Henle
curs rarely. and in proximal tubule. Therapeutic
Effect: Produces diuresis.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT PHARMACOKINETICS
Question for hypersensitivity to any corti- Route Onset Peak Duration
costeroids, components. Auscultate lung PO 30–60 min 60–120 min 4–6 hrs
sounds. IV Rapid 15–30 min 2–3 hrs

INTERVENTION/EVALUATION Completely absorbed from GI tract (ab-


Monitor for relief of symptoms. Auscul- sorption decreased in HF, nephrotic
tate lung sounds. Observe proper use of syndrome). Protein binding: 94%–96%.
medication delivery device to ensure cor- Partially metabolized in liver. Primarily
rect technique. excreted in urine. Not removed by hemo-
dialysis. Half-life: 1–1.5 hrs.
PATIENT/FAMILY TEACHING
• Improvement noted in 24 hrs, but full LIFESPAN CONSIDERATIONS
effect may take 3–7 days. • Report if no Pregnancy/Lactation: Unknown if
improvement in symptoms or if sneezing, drug is distributed in breast milk. Chil-
nasal irritation occurs. dren: Safety and efficacy not estab-
lished. Elderly: May be more sensitive
to hypotension/electrolyte effects. In-
bumetanide creased risk for circulatory collapse or
thrombolytic episode. Age-related renal
bue-met-a-nide impairment may require reduced or ex-
(Bumex, Burinex ) tended dosage interval.
j BLACK BOX ALERT jExcess INTERACTIONS
dosage can lead to profound diure-
sis with fluid and electrolyte loss. DRUG: Agents inducing hypoka-
Do not confuse bumetanide with lemia (e.g., metOLazone, hydro-
Buminate. CHLOROthiazide) may increase risk
of hypokalemia. NSAIDs (e.g., di-
uCLASSIFICATION clofenac, naproxen) may increase ef-
PHARMACOTHERAPEUTIC: Loop fect. May increase hyponatremic effect
diuretic. CLINICAL: Diuretic. of desmopressin. HERBAL: Herbals
with hypertensive properties (e.g.,
Canadian trade name Non-Crushable Drug High Alert drug
164 bumetanide
licorice, yohimbe) or hypotensive Usual Pediatric Dosage
B properties (e.g., garlic, ginger, IV, IM, PO: CHILDREN:0.015–0.1 mg/kg/
ginkgo biloba) may alter effects. dose q6–24h. Maximum: 10 mg/day. NE-
FOOD: None known. LAB VALUES: May ONATES: 0.01–0.05 mg/kg/dose q12–48h.
increase serum glucose, BUN, uric
acid; urinary phosphate. May decrease Dosage in Renal/Hepatic Impairment
serum calcium, chloride, magnesium, Use caution; contraindicated in anuria,
potassium, sodium. hepatic coma.

AVAILABILITY (Rx) SIDE EFFECTS


Injection Solution: 0.25 mg/mL. Tab- Expected: Increased urinary frequency
lets: 0.5 mg, 1 mg, 2 mg. and urine volume. Frequent (5%): Muscle
cramps, dizziness, hypotension, headache,
ADMINISTRATION/HANDLING nausea. Occasional (3%–1%): Impaired
hearing, pruritus, ECG changes, weakness,
IV hives, abdominal pain, dyspepsia, mus-
Rate of administration • May give un- culoskeletal pain, rash, nausea, vomiting.
diluted but is compatible with D5W, 0.9% Rare (less than 1%): Chest pain, ear pain,
NaCl, or lactated Ringer’s solution. • Ad- fatigue, dry mouth, premature ejaculation,
minister IV push over 1–2 min. • May impotence, nipple tenderness.
give through Y tube or 3-way stop-
cock. • May give as continuous infusion. ADVERSE EFFECTS/TOXIC
Storage • Store at room tempera-
REACTIONS
ture. • Stable for 24 hrs if diluted. Vigorous diuresis may lead to profound
water and electrolyte depletion, result-
PO ing in hypokalemia, hyponatremia, de-
• Give with food to avoid GI upset, pref- hydration, coma, circulatory collapse.
erably with breakfast (may prevent noc- Ototoxicity manifested as deafness, ver-
turia). tigo, tinnitus may occur, esp. in pts with
severe renal impairment or those taking
IV INCOMPATIBILITIES other ototoxic drugs. Blood dyscrasias,
Midazolam (Versed). acute hypotensive episodes have been
reported.
IV COMPATIBILITIES
Aztreonam (Azactam), cefepime (Maxi- NURSING CONSIDERATIONS
pime), dexmedetomidine (Precedex), BASELINE ASSESSMENT
diltiaZEM (Cardizem), DOBUTamine
(Dobutrex), furosemide (Lasix), LORaz- Obtain baseline vital signs, esp. B/P for
epam (Ativan), milrinone (Primacor), hypotension, before administration. As-
morphine, piperacillin and tazobactam sess baseline electrolytes, particularly
(Zosyn), propofol (Diprivan). for hypokalemia, hyponatremia. Assess
for edema. Observe skin turgor, mucous
INDICATIONS/ROUTES/DOSAGE membranes for hydration status. Initiate
Edema, HF
I&O, obtain baseline weight.
PO: ADULTS, ELDERLY: 0.5–2 mg 1–2 INTERVENTION/EVALUATION
times/day. May repeat in 4–5 hrs for up Continue to monitor B/P, vital signs,
to 2 doses. Maximum: 10 mg/day. electrolytes, I&O, weight. Note extent of
IV, IM: ADULTS, ELDERLY: 0.5–1 mg/dose; diuresis. Watch for changes from initial
may repeat in 2–3 hrs for up to 2 doses assessment (hypokalemia may result
(Maximum: 10 mg/day) or 0.5–2 mg/hr in muscle weakness, tremor, muscle
by continuous IV infusion. Repeat loading cramps, altered mental status, cardiac
dose before increasing infusion rate.
underlined – top prescribed drug
buprenorphine 165
arrhythmias; hyponatremia may result in USES
confusion, thirst, cold/clammy skin). Sublingual tablet: Treatment of B
PATIENT/FAMILY TEACHING opioid dependence. Implant: Main-
tenance treatment of opioid depen-
• Expect increased urinary frequency/
dence in pts who achieved/sustained
volume. • Report auditory abnormali-
prolonged clinical stability on low to
ties (e.g., sense of fullness in ears, tinni-
moderate doses of a transmucosal bu-
tus). • Eat foods high in potassium
prenorphine product for 3 months or
such as whole grains (cereals), legumes,
longer with no need for supplemental
meat, bananas, apricots, orange juice,
dosing or adjustments. Injection:
potatoes (white, sweet), raisins. • Rise
Relief of moderate to severe pain.
slowly from sitting/lying position.
Transdermal, buccal film: Moderate
to severe chronic pain requiring con-
tinuous around-the-clock opioid anal-
buprenorphine gesic for extended period. OFF-LABEL:
Injection: Heroin/opioid withdrawal in
bue-pre-nor-feen hospitalized pts.
(Belbuca, Buprenex, Butrans,
Probuphine) PRECAUTIONS
j BLACK BOX ALERT jTransder- Contraindications: Hypersensitivity to
mal, Immediate-Release, Injection: buprenorphine. Additional: Transder-
Prolonged use during pregnancy may mal patch, buccal film, immediate-
result in neonatal abstinence syn- release injection: Significant respira-
drome. Potential for abuse, misuse, tory depression, severe asthma in an un-
and diversion. Do not exceed dose
of one 20 mcg/hr patch due to risk of monitored setting or in absence of resus-
QT interval prolongation. May cause citative equipment, known or suspected
potentially life-threatening respira- GI obstruction, including paralytic ileus.
tory depression. Implant: Potential for Cautions: Hepatic/renal impairment,
implant migration, protrusion, expul- elderly, debilitated, pediatric pts, head
sion, and nerve damage associated
with insertion and removal. injury/increased intracranial pressure,
Do not confuse Buprenex with pts at risk for respiratory depression,
Bumex, or buprenorphine with hyperthyroidism, myxedema, adrenal
buPROPion. cortical insufficiency (e.g., Addison’s
disease), urethral stricture, CNS depres-
FIXED-COMBINATION(S) sion, morbid obesity, toxic psychosis,
Brunavail: buprenorphine/naloxone prostatic hypertrophy, delirium tremens,
(narcotic antagonist): 2.1 mg/0.3 mg; kyphoscoliosis, biliary tract dysfunction,
4.2 mg/0.7 mg; 6.3 mg/1 mg. acute pancreatitis, acute abdominal con-
Suboxone: buprenorphine/naloxone: 2 ditions, acute alcoholism, pts with pro-
mg/0.5 mg, 4 mg/1 mg, 8 mg/2 mg, 12 longed QT syndrome, concurrent use of
mg/3 mg. Zubsolv: buprenorphine/nal- antiarrhythmics, hypovolemia, cardiovas-
oxone: 1.4 mg/0.36 mg; 5.7 mg/1.4 mg. cular disease, ileus, bowel obstruction,
hx of seizure disorder.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Opioid
ACTION
agonist, partial agonist (Schedule Binds to mu opioid receptors within CNS.
V). CLINICAL: Opioid dependence Therapeutic Effect: Suppresses opioid
adjunct, analgesic. withdrawal symptoms, cravings. Alters pain
perception, emotional response to pain.

Canadian trade name Non-Crushable Drug High Alert drug


166 buprenorphine

PHARMACOKINETICS AVAILABILITY (Rx)


B Route Onset Peak Duration Buccal Film: 75 mcg, 150 mcg, 300 mcg,
Sublin- 15 min 1 hr 6 hrs 450 mcg, 600 mcg, 750 mcg, 900 mcg.
gual Implant: (Probuphine): Set of 4 implants,
IV Less Less than 6 hrs each containing 74.2 mg of buprenor-
than 15 1 hr phine (equivalent to 80 mg of buprenor-
min phine hydrochloride). Injection Solution:
IM 15 min 1 hr 6 hrs (Buprenex): 0.3 mg/1 mL. Tablets, Sub-
Excreted primarily in feces, with lesser lingual: 2 mg, 8 mg. Transdermal Weekly
amount eliminated in urine. Protein Patch: (Butrans): 5 mcg/hr, 7.5 mcg/hr,
binding: High. Half-life: Parenteral: 10 mcg/hr, 15 mcg/hr, 20 mcg/hr.
2–3 hrs; Sublingual: 37 hrs (increased
in hepatic impairment). ADMINISTRATION/HANDLING
LIFESPAN CONSIDERATIONS IV
Pregnancy/Lactation: Crosses pla- Reconstitution • May be diluted with
centa. Distributed in breast milk. Breast- lactated Ringer’s solution, D5W, 0.9% NaCl.
feeding not recommended. Neonatal Rate of administration • If given as
withdrawal noted in infant if mother was IV push, administer over at least 2 min.
treated with buprenorphine during preg-
nancy, with onset of withdrawal symptoms IM
generally noted on day 1, manifested as • Give deep IM into large muscle mass.
hypertonia, tremor, agitation, myoclo-
Buccal Film
nus. Apnea, bradycardia, seizures occur
rarely. Children: Safety and efficacy of Moisten inside cheek. Apply with dry
injection form not established in those finger. Press and hold in place for 5 sec.
2–12 yrs. Safety and efficacy of tablet, Keep film in place until dissolved (approx
fixed-combination form not established 30 min). Do not chew, swallow, touch, or
in pts 16 yrs or younger. Elderly: Age- move film. Do not cut/tear. Avoid areas
related hepatic impairment may require with open sores/lesions.
dosage adjustment. Sublingual
INTERACTIONS • Instruct pt to dissolve tablet(s) under
tongue; avoid swallowing (reduces drug
DRUG: CNS depressants (e.g., loraz- bioavailability). • For doses greater than
epam, morphine, zolpidem), MAOIs 2 tablets, either place all tablets at once or
(e.g., phenelzine, selegiline) may 2 tablets at a time under the tongue.
increase CNS or respiratory depression, Storage • Store parenteral form at
hypotension. CYP3A4 inhibitors (e.g., room temperature. • Protect from pro-
clarithromycin, ketoconazole, rito- longed exposure to light. • Store tab-
navir) may increase plasma concentra- lets at room temperature.
tion. CYP3A4 inducers (e.g., carBA-
Mazepine, phenytoin, rifAMPin) may Transdermal
cause increased clearance of buprenor- • Apply to clean, dry, intact, nonirritated,
phine. HERBAL: Herbals with seda- hairless skin of upper outer arm, upper
tive properties (e.g., chamomile, chest, upper back, or side of chest. Hair at
kava kava, valerian) may increase CNS application site should be clipped; do not
depression. St. John’s wort may de- shave. • Clean site with clear water and
crease concentration/effect. FOOD: None allow to dry. Do not use soaps, alcohol,
known. LAB VALUES: May increase se- oils (may increase absorption). Press
rum amylase, lipase. patch in place and hold for 15 sec-

underlined – top prescribed drug


buprenorphine 167
onds. • Wait minimum of 21 days before Buccal: ADULTS, ELDERLY: (OPIOID NA-
reapplying to same site. • Avoid exposing IVE):Initially, 75 mcg once or q12h for 4 B
patch to external heat sources. Incidental days, then 150 mcg q12h. (OPIOID EXPERI-
exposure to water is acceptable. Patch may ENCED): Taper current opioid to no more
be taped in place with first-aid tape. • If than 30 mg oral morphine equivalent.
patch falls off during 7-day dosing interval, Based on opioid dose before taper-
apply new patch to a different skin site. ing: 75 mcg once daily or q12h for less
than 30 mg; 150 mcg q12h for 30–89
IV INCOMPATIBILITIES mg; 300 mcg q12h for 90–160 mg.
DiazePAM (Valium), furosemide (Lasix),
LORazepam (Ativan). Dosage in Renal Impairment
Use caution.
IV COMPATIBILITIES Dosage in Hepatic Impairment
Allopurinol (Aloprim, Zyloprim), aztreo- Injection: Use caution.
nam (Azactam), cefepime (Maxipime), Transdermal: No adjustment.
diphenhydrAMINE (Benadryl), granisetron
(Kytril), haloperidol (Haldol), heparin, SIDE EFFECTS
linezolid (Zyvox), midazolam (Versed), Frequent (67%–10%): Sedation, dizziness,
piperacillin/tazobactam (Zosyn), prometh- nausea. Butrans (more than 5%): Nausea,
azine (Phenergan), propofol (Diprivan). headache, pruritus at application site,
dizziness, rash, vomiting, constipation,
INDICATIONS/ROUTES/DOSAGE dry mouth. Implant (more than 5%): Head-
Opioid Dependence ache, nausea, vomiting, constipation. Oc-
Sublingual: ADULTS, CHILDREN 13 YRS casional (5%–1%): Headache, hypoten-
AND OLDER: 8 mg on day 1, then 16 mg sion, vomiting, miosis, diaphoresis. Rare
on day 2 and subsequent induction days. (less than 1%): Dry mouth, pallor, visual
Range: 12–16 mg/day (usually over abnormalities, injection site reaction.
3–4 days). Maintenance: Target dose
12–16 mg/day. Pts should be switched to ADVERSE EFFECTS/TOXIC
buprenorphine/naloxone combination for REACTIONS
maintenance and unsupervised therapy. Overdosage results in cold, clammy skin,
Implant: Four implants inserted subder- weakness, confusion, severe respiratory
mally in upper arm for 6 mos of treatment. depression, cyanosis, pinpoint pupils,
seizures, extreme drowsiness progress-
Moderate to Severe Acute Pain ing to stupor, coma.
IM/IV: ADULTS, ELDERLY, CHILDREN 13
YRS AND OLDER: 0.3 mg (1 mL) q6–8h NURSING CONSIDERATIONS
prn; may repeat once 30–60 min after
initial dose. CHILDREN 2–12 YRS: 2–6 BASELINE ASSESSMENT
mcg/kg q4–6h prn. Obtain baseline B/P, pulse rate. Assess men-
tal status, alertness. Assess type, location,
Moderate to Severe Chronic Pain intensity of pain. Obtain history of pt’s last
Transdermal: ADULTS, ELDERLY: (OPIOID opioid use. Assess for early signs of with-
NAÏVE): Initial dose 5 mcg/hr once q7days. drawal symptoms before initiating therapy.
(OPIOID EXPERIENCED): Discontinue all other
INTERVENTION/EVALUATION
around-the-clock opioid medications. Ini-
tial dose based on morphine equivalent Monitor for change in respirations, B/P,
dose: (Less than 30 mg): Initially 5 mcg/ rate/quality of pulse, mental status. As-
hr q7days. (30–80 mg): 10 mcg/hr q7days. sess lab results. Initiate deep breathing,
(Greater than 80 mg): 20 mcg/hr q7days. coughing exercises, particularly in pts
with pulmonary impairment. Assess for

Canadian trade name Non-Crushable Drug High Alert drug


168 buPROPion
clinical improvement; record onset of of anorexia nervosa or bulimia, seizure
B relief of pain. Monitor strictly for compli- disorder, use of MAO inhibitors (concur-
ance, signs of abuse or misuse. rently or within 14 days of discontinuing
PATIENT/FAMILY TEACHING
either bupropion or the MAOI); pts un-
dergoing abrupt discontinuation of alco-
• Change positions slowly to avoid dizzi- hol or sedatives. Initiation of buPROPion
ness, orthostatic hypotension. • Avoid in pts receiving linezolid or IV methylene
tasks that require alertness, motor skills blue. Aplenzin, Forfivo XL, Wellbutrin
until response to drug is estab- XL (additional): Conditions increasing
lished. • Avoid alcohol, sedatives, anti- seizure risk, severe head injury, stroke,
depressants, tranquilizers. CNS tumor/infection. Forfivo XL (addi-
tional): Pts receiving other dosage forms
of bupropion. Cautions: History of sei-
zure, cranial or head trauma, cardiovas-
buPROPion cular disease, history of hypertension or
coronary artery disease, elderly, pts at high
bue-proe-pee-on risk for suicide, renal/hepatic impairment.
(Aplenzin, Forfivo XL, Wellbutrin SR, Concurrent use of antipsychotics, antide-
Wellbutrin XL, Zyban) pressants, theophylline, steroids, stimu-
j BLACK BOX ALERT j lants, hypoglycemic agents, excessive use
Increased risk of suicidal thinking of alcohol, sedatives/hypnotics, opioids.
and behavior in children, adoles-
cents, young adults 18–24 yrs with
major depressive disorder, other ACTION
psychiatric disorders. Agitation, Blocks reuptake of neurotransmitters,
hostility, depressed mood also (DOPamine, norepinephrine) at CNS
reported. Use in smoking cessation presynaptic membranes. Therapeutic
may cause serious neuropsychiat-
ric events. Effect: Relieves depression. Eliminates
Do not confuse Aplenzin with nicotine withdrawal symptoms.
Relenza, buPROPion with
PHARMACOKINETICS
busPIRone, Wellbutrin SR with
Wellbutrin XL, or Zyban with Rapidly absorbed from GI tract. Protein
Diovan or Zagam. binding: 84%. Crosses the blood-brain
barrier. Metabolized in liver. Primarily
uCLASSIFICATION excreted in urine. Half-life: 14 hrs.
PHARMACOTHERAPEUTIC: Dopa-
LIFESPAN CONSIDERATIONS
mine/norepinephrine reuptake in-
hibitor. CLINICAL: Antidepressant, Pregnancy/Lactation: Unknown if
smoking cessation aid. drug crosses placenta or is distributed in
breast milk. Children: More sensitive to
increased dosage, toxicity; increased risk
USES of suicidal ideation, worsening of depres-
Treatment of major depressive disor- sion. Safety and efficacy not established.
der (MDD), seasonal affective disorder Elderly: More sensitive to anticholiner-
(SAD). Zyban assists in smoking cessa- gic, sedative, cardiovascular effects. Age-
tion. OFF-LABEL: Treatment of ADHD in related renal impairment may require
adults, children. Depression associated dosage adjustment.
with bipolar disorder.
INTERACTIONS
PRECAUTIONS DRUG: CNS depressants (e.g., al-
Hypersensitivity
Contraindications: to cohol, morphine, oxyCODONE,
buPROPion. Current or prior diagnosis zolpidem) may increase CNS depres-

underlined – top prescribed drug


buPROPion 169
sant effect. MAOIs (e.g., phenelzine, no clinical improvement after 2 wks, may
selegiline) may increase hypertensive increase to 450 mg once daily. Maxi- B
effect. May decrease concentration of mum: 450 mg/day. (Aplenzin): Ini-
tamoxifen. May increase concentra- tially, 174 mg once daily in morning; may
tion of aripiprazole, brexpiprazole, increase as soon as 4 days to 348 mg/day.
iloperidone, metoclopramide, thio-
ridazine. May increase adverse effects Smoking Cessation
of citalopram, vortioxetine. HERBAL: PO: ADULTS, ELDERLY: (Zyban): Initially,
Herbals with sedative properties 150 mg/day for 3 days, then 150 mg twice
(e.g., chamomile, kava kava, va- daily for 7–12 wks.
lerian) may increase CNS depression.
SAD
FOOD: None known. LAB VALUES: May
PO: ADULTS, ELDERLY: (Wellbutrin XL):
decrease WBC.
150 mg/day for 1 wk, then 300 mg/day.
AVAILABILITY (Rx) Begin in autumn (Sept–Nov). End of
Tablets: 75 mg, 100 mg. treatment begins in spring (Mar–Apr)
by decreasing dose to 150 mg/day for 2
Tablets, Extended-Release (24 wks before discontinuation. (Aplenzin):
hr): (Aplenzin): 174 mg, 348 mg, 522 mg 174 mg once daily. May increase after 1
(Forfivo XL): 450 mg (Wellbutrin XL): 150 wk to 348 mg once daily.
mg, 300 mg. Tablets, Sustained-Release (12
hr): (Wellbutrin SR): 100 mg, 150 mg, 200 Dosage in Renal Impairment
mg; (Zyban): 150 mg. Use caution.
ADMINISTRATION/HANDLING Dosage in Hepatic Impairment
PO Mild to moderate impairment: Use
• Give without regard to food (give with caution, reduce dosage. Severe im-
food if GI irritation occurs). • Give at pairment: Use extreme caution. Maxi-
least 4-hr interval for immediate onset and mum: (Aplenzin): 174 mg every other
8-hr interval for sustained-release tablet to day. (Wellbutrin): 75 mg/day. (Wellbutrin
avoid seizures. • Give Aplenzin once daily SR): 100 mg/day or 150 mg every other
in the morning. • Avoid bedtime dosage day. (Wellbutrin XL): 150 mg every other
(decreases risk of insomnia). • Do not day. (Zyban): 150 mg every other day.
break, crush, dissolve, or divide sustained-,
extended-release preparations. SIDE EFFECTS
Frequent (32%–18%): Constipation, weight
INDICATIONS/ROUTES/DOSAGE gain or loss, nausea, vomiting, anorexia,
Depression dry mouth, headache, diaphoresis,
PO: (Immediate-Release): ADULTS, tremor, sedation, insomnia, dizziness,
ELDERLY: Initially, 100 mg twice daily. agitation. Occasional (10%–5%): Diar-
May increase to 100 mg 3 times/day no rhea, akinesia, blurred vision, tachycar-
sooner than 3 days after beginning ther- dia, confusion, hostility, fatigue.
apy. Maximum: 150 mg 3 times/day.
PO: (Sustained-Release): ADULTS, EL- ADVERSE EFFECTS/TOXIC
DERLY: Initially, 150 mg/day as a single REACTIONS
dose in the morning. May increase to Risk of seizures increases in pts taking
150 mg twice daily as early as day 4 after more than 150 mg/dose; in pts with history
beginning therapy. Maximum: 400 mg/ of bulimia, seizure disorders, discontinu-
day in 2 divided doses. ing drugs that may lower seizure threshold.
PO: (Extended-Release): ADULTS,
ELDERLY:150 mg once daily. May increase
to 300 mg once daily as early as day 4. If

Canadian trade name Non-Crushable Drug High Alert drug


170 busPIRone

NURSING CONSIDERATIONS to treat depression. Concomitant use of


B MAOIs within 14 days of discontinuing
BASELINE ASSESSMENT buspirone. Initiation of buspirone in pts
Assess psychological status, thought con- receiving IV methylene blue or linezolid.
tent, suicidal tendencies, appearance. Cautions: Concurrent use of MAOIs, se-
For pts on long-term therapy, hepatic/ vere hepatic/renal impairment (not rec-
renal function tests should be performed ommended).
periodically.
ACTION
INTERVENTION/EVALUATION Exact mechanism of action unknown.
Supervise suicidal-risk pt closely during Binds to serotonin, DOPamine at presyn-
early therapy and dose changes (as de- aptic neurotransmitter receptors in CNS.
pression lessens, energy level improves, Therapeutic Effect: Produces anxio-
increasing suicide potential). Assess ap- lytic effect.
pearance, behavior, speech pattern, level
of interest, mood changes. PHARMACOKINETICS
PATIENT/FAMILY TEACHING
Rapidly and completely absorbed from
GI tract. Protein binding: 95%. Metabo-
• Full therapeutic effect may be noted in lized in liver. Primarily excreted in urine.
4 wks. • Avoid tasks that require alert- Not removed by hemodialysis. Half-
ness, motor skills until response to drug life: 2–3 hrs.
is established. • Report signs/symp-
toms of seizure, worsening depression, LIFESPAN CONSIDERATIONS
suicidal ideation, unusual behavioral Pregnancy/Lactation: Unknown if
changes. • Avoid alcohol. • Do not drug crosses placenta or is distributed
chew, crush, dissolve, or divide sus- in breast milk. Children: Safety and ef-
tained-, extended-release tablets. ficacy not established. Elderly: No age-
related precautions noted.

busPIRone INTERACTIONS
DRUG: CNS depressants (e.g., alco-
bue-spye-rone hol, morphine, oxyCODONE, zol-
Do not confuse busPIRone with pidem) may increase CNS depressant
buPROPion. effect. May increase adverse effects of
MAOIs (e.g., phenelzine, selegiline).
uCLASSIFICATION May increase serotonergic effects of
PHARMACOTHERAPEUTIC: Nonbar- SSRIs (e.g., citalopram, FLUoxetine,
biturate. CLINICAL: Antianxiety. sertraline). CYP3A4 inhibitors (e.g.,
erythromycin, ketoconazole) may in-
crease concentration/effect. CYP3A4 in-
USES ducers (e.g., rifAMPin) may decrease
Management of anxiety disorders. concentration/effect. HERBAL: Herb-
Short-term relief of symptoms of anxiety. als with sedative properties (e.g.,
OFF-LABEL: Augmenting medication for chamomile, kava kava, valerian)
antidepressants. may increase CNS depression. St. John’s
wort may decrease concentration/ef-
PRECAUTIONS fect. FOOD: Grapefruit products may
Contraindications: Hypersensitivity to increase concentration, risk of toxicity.
busPIRone. Concomitant use of MAOIs LAB VALUES: May produce false-positive
intended to treat depression or within urine metanephrine/catecholamine assay
14 days of discontinuing MAOIs intended test.

underlined – top prescribed drug


busPIRone 171

AVAILABILITY (Rx) withdrawal syndrome. Overdose may


Tablets: 5 mg, 7.5 mg, 10 mg, 15 mg, produce severe nausea, vomiting, dizzi- B
30 mg. ness, drowsiness, abdominal distention,
excessive pupil constriction.
ADMINISTRATION/HANDLING
NURSING CONSIDERATIONS
PO
• Give without regard to food. Must be BASELINE ASSESSMENT
consistent. Assess degree/manifestations of anxiety.
Offer emotional support. Assess mo-
INDICATIONS/ROUTES/DOSAGE tor responses (agitation, trembling,
Anxiety Disorders tension), autonomic responses (cold,
PO: ADULTS, ELDERLY: Initially, 10–15 clammy hands; diaphoresis).
mg/day in 2–3 divided doses. May in-
crease every 2–3 days in increments of INTERVENTION/EVALUATION
2.5 mg twice daily. Maintenance: 10– For pts on long-term therapy, CBC, LFT,
15 mg twice daily. Maximum: 30 mg renal function tests should be performed
twice daily. periodically. Assist with ambulation if
drowsiness, dizziness occur. Evaluate for
Dosage in Renal/Hepatic Impairment therapeutic response: calm facial expres-
Not recommended in severe impairment. sion, decreased restlessness, lessened
SIDE EFFECTS insomnia, mental status.
Frequent (12%–6%): Dizziness, drowsi- PATIENT/FAMILY TEACHING
ness, nausea, headache. Occasional • Improvement may be noted in 7–10
(5%–2%): Nervousness, fatigue, insom- days, but optimum therapeutic effect
nia, dry mouth, light-headedness, mood generally takes 3–4 wks. • Drowsiness
swings, blurred vision, poor concentra- usually disappears during continued
tion, diarrhea, paresthesia. Rare: Muscle therapy. • If dizziness occurs, slowly
pain/stiffness, nightmares, chest pain, go from lying to standing. • Avoid
involuntary movements. tasks that require alertness, motor skills
until response to drug is estab-
ADVERSE EFFECTS/TOXIC lished. • Avoid alcohol, grapefruit
REACTIONS products. • Be consistent in taking
No evidence of drug tolerance, psy- with regard to food.
chological or physical dependence,

Canadian trade name Non-Crushable Drug High Alert drug


172 cabazitaxel
microtubule depolymerization/cell divi-
cabazitaxel sion. Therapeutic Effect: Arrests the cell
cycle, inhibiting tumor proliferation.
C ka-baz-i-tax-el
(Jevtana) PHARMACOKINETICS
j BLACK BOX ALERT jAll pts Widely distributed. Metabolized in liver.
should be premedicated with a Protein binding: 89%–92%. Excreted
corticosteroid, an antihistamine, in feces (76%), urine (3.7%). Half-
and an H2 serum antagonist prior to
infusion. Severe hypersensitivity re- life: 95 hrs.
actions have occurred. Immediately
discontinue infusion and give ap- LIFESPAN CONSIDERATIONS
propriate treatment if hypersensitiv- Pregnancy/Lactation: May cause fetal
ity reaction occurs. Neutropenic harm. Crosses placental barrier. Breast­
deaths reported. CBC, particularly
ANC, should be obtained prior to feeding not recommended. Children:
and during treatment. Do not ad- Safety and efficacy not established. El-
minister with neutrophil count 1,500 derly: Pts 65 yrs and older have 5%
cells/mm3 or less. greater risk of developing neutropenia,
Do not confuse cabazitaxel with fatigue, dizziness, fever, urinary tract in-
PACLitaxel or Paxil, or Jevtana fection, dehydration.
with Januvia, Levitra, or Sentra.
INTERACTIONS
uCLASSIFICATION
DRUG: Strong CYP3A4 inhibitors
PHARMACOTHERAPEUTIC: Microtu- (e.g., atazanavir, clarithromycin, ke-
bule inhibitor. CLINICAL: Antineo- toconazole, ritonavir) may increase
plastic. concentration/effect; avoid use. Strong
CYP3A4 inducers (e.g., carBAMaze-
pine, PHENobarbital, phenytoin,
USES rifAMPin) may decrease cabazitaxel
Used in combination with predniSONE concentration effects. Live virus vac-
for treatment of castration-resistant met- cine may potentiate virus replication,
astatic prostate cancer previously treated increase vaccine’s side effects, decrease
with a DOCEtaxel-containing regimen. response to vaccine. HERBAL: Echina-
cea may decrease therapeutic effect. St.
PRECAUTIONS John’s wort may decrease concentration/
Contraindications: Hypersensitivity to ca- effect. FOOD: Grapefruit products may
bazitaxel. Severe hepatic impairment (total increase concentration/effects. LAB VAL-
serum bilirubin greater than 3 times upper UES: May increase serum bilirubin. May
limit of normal [ULN]). Neutrophil count of decrease Hgb, Hct, neutrophils, platelets.
1,500 cells/mm3 or less, history of hyper-
sensitivity to polysorbate 80. Caution: Mild AVAILABILITY (Rx)
to moderate hepatic impairment (bilirubin Injection: 60 mg/1.5 mL
equal to or less than 3 times ULN), elderly,
pregnancy, renal impairment (CrCl less ADMINISTRATION/HANDLING
than 30 mL/min). Pts at risk for develop- b ALERT c Wear gloves during prepa-
ing GI complications (e.g., GI ulceration, ration, handling. Two-step dilution pro-
concomitant use of NSAIDs). cess must be performed under aseptic
ACTION conditions to prepare second (final) in-
fusion solution. Medication undergoes
Binds to tubulin to promote assembly into two dilutions. After second dilution, ad-
microtubules and inhibits disassembly, ministration should be initiated within
which stabilizes microtubules. Inhibits 30 min.
underlined – top prescribed drug
cabazitaxel 173
Reconstitution Dose Modification
Step 1, first dilution • Each vial of Grade 3 neutropenia, febrile neutro-
cabazitaxel contains 60 mg/1.5 mL; penia, Grade 3 or persistent diarrhea,
must first be mixed with entire contents neuropathy: Reduce dosage to 20 mg/m2 C
of supplied diluent. • Once reconsti- after treatment interruption.
tuted, solution contains 10 mg/mL of
cabazitaxel. • When transferring dilu- Dosage with Strong CYP3A Inhibitors
ent, direct needle onto inside vial wall Consider dose reduction by 25%.
and inject slowly to limit foam-
Dosage in Renal Impairment
ing. • Remove syringe and needle,
then gently mix initial diluted solution CrCl less than 15 mL/min: Use caution.
by repeated inversions for at least 45 sec Dosage in Hepatic Impairment
to ensure full mixing of drug and dilu- Mild impairment: 20 mg/m2. Moder-
ent. • Do not shake. • Allow any foam ate impairment: 15 mg/m2. Severe
to dissipate. impairment: Contraindicated.
Step 2, final dilution • Withdraw
recommended dose and further dilute SIDE EFFECTS
with 250 mL 0.9% NaCl or D5W. • If Frequent (47%–16%): Diarrhea, fatigue,
dose greater than 65 mg is required, use nausea, vomiting, constipation, esthesia,
larger volume of 0.9% NaCl or D5W so abdominal pain, anorexia, back pain.
that concentration of 0.26 mg/mL is not Occasional (13%–5%): Peripheral neu-
exceeded. • Concentration of final di- ropathy, fever, dyspnea, cough, arthralgia,
luted solution should be between 0.10 dysgeusia, dyspepsia, alopecia, periph-
and 0.26 mg/mL. eral edema, weight decrease, urinary tract
Rate of administration • Infuse over infection, dizziness, headache, muscle
1 hr using in-line 0.22-micron filter. spasm, dysuria, hematuria, mucosal in-
Storage • Store vials at room temper- flammation, dehydration.
ature. • First dilution solution stable
for 30 min. • Final diluted solution ADVERSE EFFECTS/TOXIC
stable for 8 hrs at room temperature or REACTIONS
24 hrs if refrigerated. Hypersensitivity reaction may include
INDICATIONS/ROUTES/DOSAGE generalized rash, erythema, hypotension,
bronchospasm. 94% of pts develop Grade
b ALERT c Antihistamine (dexchlor- 1–4 neutropenia and associated complica-
pheniramine 5 mg, diphenhydrAMINE 25 tions including anemia, thrombocytopenia,
mg, or equivalent antihistamine), corti- sepsis. GI abnormalities, hypertension, ar-
costeroid (dexamethasone 8 mg or rhythmias, renal failure may occur.
equivalent), and H2 antagonist (raNITI-
dine 50 mg or equivalent H2 antagonist) NURSING CONSIDERATIONS
should be given at least 30 min prior to
each dose to reduce risk/severity of hy- BASELINE ASSESSMENT
persensitivity. Obtain ANC, CBC, BMP, LFT, serum testos-
terone. Assess ANC, CBC prior to each in-
Metastatic Prostate Cancer fusion. Question history of hypersensitivity
b ALERT c Monitoring of CBC is es- reaction; renal/hepatic impairment; intol-
sential on wkly basis during cycle 1 and erance to corticosteroids. Receive full med-
before each treatment cycle thereafter so ication history and screen for interactions.
that the dose can be adjusted.
IV infusion: ADULTS, ELDERLY: 20–25 INTERVENTION/EVALUATION
mg/m2 given as 1-hr infusion q3wks in Monitor CBC, ANC on wkly basis during
combination with predniSONE. cycle 1 and before each treatment cycle

Canadian trade name Non-Crushable Drug High Alert drug


174 calcitonin
thereafter; do not administer if ANC less ACTION
than 1,500 cells/mm3. Monitor serum Antagonizes effects of parathyroid hor-
ALT, AST, renal function. Monitor for hy- mone. Increases jejunal secretion of wa-
C persensitivity reaction (rash, erythema, ter, sodium, potassium, chloride. Inhibits
dyspnea). Encourage adequate fluid in- osteoclast bone resorption. Promotes
take. Monitor daily pattern of bowel activ- renal excretion of calcium, phosphate, so-
ity, stool consistency. Offer antiemetics if dium, magnesium, potassium by decreasing
nausea, vomiting occur. Closely monitor tubular reabsorption. Therapeutic Effect:
for signs/symptoms of neutropenia. Regulates serum calcium concentrations.
PATIENT/FAMILY TEACHING
PHARMACOKINETICS
• Report fever, chills, persistent sore
Nasal form rapidly absorbed. Injection
throat, unusual bruising/bleeding, pale
form rapidly metabolized primarily in kid-
skin, fatigue. • Avoid tasks that require
neys. Primarily excreted in urine. Half-life:
alertness, motor skills until response to
Nasal: 43 min; Injection: 70–90 min.
drug is established. • Maintain strict
oral hygiene. • Do not have immuniza- LIFESPAN CONSIDERATIONS
tions without physician approval (drug
Pregnancy/Lactation: Does not cross
lowers body’s resistance). • Avoid
placenta; unknown if distributed in
those who have received a live virus vac-
breast milk. Safe usage during lactation
cine. • Avoid crowds, those with cough,
not established (inhibits lactation in
sneezing. • Avoid grapefruit prod-
animals). Children: Safety and efficacy
ucts. • Diarrhea may cause dehydra-
not established. Elderly: No age-related
tion; drink plenty of fluids.
precautions noted.
INTERACTIONS
calcitonin DRUG: May decrease lithium concentra-
tion/effects. May increase concentration/
kal-si-toe-nin effect of zoledronic acid. HERBAL: None
(Calcimar , Miacalcin) significant. FOOD: None known. LAB VAL-
Do not confuse calcitonin with UES: None significant.
calcitriol, or Miacalcin with
Micatin. AVAILABILITY (Rx)
Injection Solution: (Miacalcin): 200 units/
uCLASSIFICATION mL. Nasal Spray: (Miacalcin Nasal): 200
PHARMACOTHERAPEUTIC: Synthetic units/activation.
hormone. CLINICAL: Calcium regu-
lator, bone resorption inhibitor. ADMINISTRATION/HANDLING
IM, SQ
• IM route preferred if injection volume
USES greater than 2 mL. Subcutaneous injec-
Parenteral: Treatment of Paget’s disease tion for outpatient self-administration
of bone, hypercalcemia, postmenopausal unless volume greater than 2 mL. • Skin
osteoporosis in women greater than 5 yrs test should be performed before therapy
postmenopause. Intranasal: Postmeno- in pts suspected of sensitivity to calcito-
pausal osteoporosis in women more than nin. • Bedtime administration may re-
5 yrs postmenopause. duce nausea, flushing.
PRECAUTIONS Intranasal
Contraindications: Hypersensitivity to cal- • Refrigerate unopened nasal spray. Store
citonin, salmon. Cautions: None known. at room temperature after initial use.
underlined – top prescribed drug
calcium acetate 175
• Instruct pt to clear nasal passages. ADVERSE EFFECTS/TOXIC
• Tilt head slightly forward. • Insert REACTIONS
spray tip into nostril, pointing toward nasal Pts with a protein allergy may develop a
passages, away from nasal septum. hypersensitivity reaction (rash, dyspnea, C
• Spray into one nostril while pt holds hypotension, tachycardia).
other nostril closed and concurrently in-
spires through nose to deliver medication NURSING CONSIDERATIONS
as high into nasal passage as possible. Spray
into one nostril daily. • Discard after 30 BASELINE ASSESSMENT
doses. Obtain baseline serum electrolyte levels.
INDICATIONS/ROUTES/DOSAGE INTERVENTION/EVALUATION
Skin Testing Before Treatment in Pts with Ensure rotation of injection sites; check
Suspected Sensitivity to Calcitonin-Salmon for inflammation. Assess vertebral bone
Note: A detailed skin testing protocol is mass (document stabilization/improve-
available from the manufacturer. ment). Assess for allergic response: rash,
urticaria, swelling, dyspnea, tachycardia,
Paget’s Disease
hypotension. Monitor serum electrolytes,
IM, SQ: ADULTS, ELDERLY: 100 units/day.
calcium, alkaline phosphatase.
Postmenopausal Osteoporosis PATIENT/FAMILY TEACHING
IM, SQ: ADULTS, ELDERLY: 100 units daily
• Instruct pt/family on aseptic tech-
with adequate calcium and vitamin D nique, proper injection method of subcu-
intake. taneous medication, including rotation of
Intranasal: ADULTS, ELDERLY: 200 units/
sites, proper administration of nasal
day as a single spray in one nostril, alter- medication. • Nausea is transient and
nating nostrils daily. usually decreases over time. • Immedi-
Hypercalcemia ately report rash, itching, shortness of
IM, SQ: ADULTS, ELDERLY: Initially, 4 breath, significant nasal irritation.
units/kg q12h; may increase to 8 units/kg • Improvement in biochemical abnor-
q12h if no response in 2 days; may further malities and bone pain usually occurs in
increase to 8 units/kg q6–12h. the first few months of treatment. • Im-
provement of neurologic lesions may
Dosage in Renal/Hepatic Impairment take more than a year.
No dose adjustment.
SIDE EFFECTS
Frequent: IM, SQ (10%): Nausea (may
calcium acetate
occur soon after injection; usually dimin- (Eliphos, PhosLo)
ishes with continued therapy), inflam-
mation at injection site. Nasal (12%–
10%): Rhinitis, nasal irritation, redness, calcium carbonate
mucosal lesions. Occasional: IM, SQ
(5%–2%): Flushing of face, hands. Na- (Apo-Cal , Caltrate 600 , OsCal
sal (5%–3%): Back pain, arthralgia, , Titralac, Tums)
epistaxis, headache. Rare: IM, SQ: Epi-
gastric discomfort, dry mouth, diarrhea, calcium chloride
flatulence. Nasal: Itching of earlobes,
pedal edema, rash, diaphoresis. (Cal-Citrate, Citracal, Osteocit )

Canadian trade name Non-Crushable Drug High Alert drug


176 calcium glubionate

calcium glubionate brane and capillary permeability. Assists in


regulating release/storage of hormones/
neurotransmitters. Neutralizes/reduces
C calcium gluconate gastric acid (increases pH). Calcium ac-
etate: Binds with dietary phosphate, form-
kal-si-um ing insoluble calcium phosphate. Calcium
Do not confuse Citracal with chloride, calcium gluconate: Mod-
Citrucel, OsCal with Asacol, or erates nerve and muscle performance
PhosLo with Prosom. by regulating action potential excitation
threshold. Therapeutic Effect: Replaces
uCLASSIFICATION calcium in deficiency states; controls hy-
PHARMACOTHERAPEUTIC: Electro- perphosphatemia in end-stage renal dis-
lyte replenisher. CLINICAL: Antacid, ease; relieves heartburn, indigestion.
antihypocalcemic, antihyperkalemic,
antihypermagnesemic, antihyperphos- PHARMACOKINETICS
phatemic. Moderately absorbed from small intes-
tine (absorption depends on presence
of vitamin D metabolites, pH). Primarily
USES eliminated in feces.
Parenteral (calcium chloride): Treat-
ment of hypocalcemia and conditions sec- LIFESPAN CONSIDERATIONS
ondary to hypocalcemia (e.g., seizures, Pregnancy/Lactation: Distributed in
arrhythmias), emergency treatment of breast milk. Unknown whether calcium
severe hypermagnesemia; (calcium glu- chloride or calcium gluconate is dis-
conate): Treatment of hypocalcemia and tributed in breast milk. Children: Risk
conditions secondary to hypocalcemia of extreme irritation, possible tissue
(e.g., seizures, arrhythmias). Calcium necrosis or sloughing with IV calcium
carbonate: Antacid, dietary supplement. preparations. Restrict IV use due to
Calcium acetate: Controls hyperphos- small vasculature. Elderly: Oral ab-
phatemia in end-stage renal disease. OFF- sorption may be decreased.
LABEL (Calcium chloride): Calcium
channel blocker overdose, severe hyper- INTERACTIONS
kalemia, malignant arrhythmias associ- DRUG: Hypercalcemia may increase
ated with hypermagnesemia. digoxin toxicity. Oral form may de-
crease absorption of bisphospho-
PRECAUTIONS nates (e.g., risedronate), calcium
Contraindications: Hypersensitivity to cal- channel blockers (e.g., amLO-
cium formulation. All preparations: Cal- DIPine, dilTIAZem, verapamil),
cium-based renal calculi, hypercalcemia, tetracycline derivatives, thyroid
ventricular fibrillation. Calcium chloride: products. HERBAL: None significant.
Digoxin toxicity. Calcium gluconate: Ne- FOOD: Food may increase calcium ab-
onates: Concurrent IV use with cefTRIAX- sorption. LAB VALUES: May increase
one. Cautions: Chronic renal impairment, serum pH, calcium, gastrin. May de-
hypokalemia, concurrent use with digoxin. crease serum phosphate, potassium.
ACTION AVAILABILITY (Rx)
Essential for function, integrity of nervous, Calcium Acetate (667 mg = 169 mg
muscular, skeletal systems. Plays an impor- calcium)
tant role in normal cardiac/renal function, Capsules: 667 mg. Tablets: (Eliphos):
respiration, blood coagulation, cell mem- 667 mg.

underlined – top prescribed drug


calcium glubionate 177
Calcium Carbonate (1 g = 400 mg calcium) meals with plenty of water (give with meals
Tablets: 500 mg, 600 mg, 1,250 mg, if used for phosphate binding). Instruct pt
1,500 mg. Tablets (Chewable): 500 mg, to thoroughly chew chewable tablets before
750 mg, 1,000 mg. swallowing. C
Calcium Chloride
Injection Solution: 10% (100 mg/mL) IV INCOMPATIBILITIES
equivalent to 27.2 mg elemental calcium Calcium chloride: Amphotericin B
per mL. complex (Abelcet, AmBisome, Ampho-
Calcium Gluconate (1 g = 93 mg calcium) tec), pantoprazole (Protonix), phos-
Injection Solution: 10%. phate-containing solutions, propofol (Di-
privan), sodium bicarbonate. Calcium
ADMINISTRATION/HANDLING gluconate: Amphotericin B complex
IV (Abelcet, AmBisome, Amphotec), fluco-
Dilution: (Calcium Chloride): May give
nazole (Diflucan).
undiluted or may dilute with 0.9% NaCl IV COMPATIBILITIES
or Sterile Water for Injection. (Calcium
Gluconate): May give undiluted or may
Calcium chloride: Amikacin (Amikin),
dilute with 100 mL 0.9% NaCl or D5W. DOBUTamine (Dobutrex), lidocaine, mil-
Rate of administration: (Calcium
rinone (Primacor), morphine, norepi-
Chloride): Note: Rapid administration
nephrine (Levophed). Calcium gluco-
may produce bradycardia, metallic/chalky nate: Ampicillin, aztreonam (Azactam),
taste, hypotension, sensation of heart, pe- ceFAZolin (Ancef), cefepime (Maxip-
ripheral vasodilation. • IV push: Infuse ime), ciprofloxacin (Cipro), DOBUTa-
slowly at maximum rate of 50–100 mg/ mine (Dobutrex), enalapril (Vasotec),
min (in cardiac arrest, may administer famotidine (Pepcid), furosemide (Lasix),
over 10–20 sec). • IV infusion: Dilute heparin, lidocaine, lipids, magnesium
to maximum final concentration of 20 mg/ sulfate, meropenem (Merrem IV), mid-
mL and infuse over 1 hr or no faster than azolam (Versed), milrinone (Primacor),
45–90 mg/kg/hr. Give via a central line. norepinephrine (Levophed), piperacillin
Do NOT use scalp, small hand or foot and tazobactam (Zosyn), potassium chlo-
veins. Stop infusion if pt complains of pain ride, propofol (Diprivan).
or discomfort. (Calcium Gluconate): INDICATIONS/ROUTES/DOSAGE
Note: Rapid administration may pro-
Hyperphosphatemia
duce vasodilation, hypotension, arrhyth-
PO: (Calcium Acetate): ADULTS, EL-
mias, syncope, cardiac arrest. • IV
push: Infuse slowly over 3–5 min or DERLY: Initially, 1334 mg 3 times/day
at maximum rate of 50–100 mg/min with meals. May increase gradually (q2–
(in cardiac arrest, may administer over 3wks) to decrease serum phosphate level
10–20 sec). • IV infusion: Dilute 1–2 to less than 6 mg/dL as long as hyper-
g in 100 mL 0.9% NaCl or D5W and infuse calcemia does not develop. Usual dose:
over 1 hr. 2,001–2,668 mg with each meal.
Storage • Store at room tempera- Hypocalcemia
ture. • Once diluted, stable for 24 hrs IV: (Calcium Chloride): ADULTS, EL-
at room temperature. DERLY: (Acute, symptomatic): 200–
PO 1,000 mg at intervals of q1–3days. (Se-
(Calcium Acetate): Administer with vere, symptomatic): 1 g over 10 min; may
plenty of fluids during meals to optimize repeat q60min until symptoms resolve.
effectiveness. (Calcium Carbonate): Ad- CHILDREN, NEONATES: 2.7–5 mg/kg q4–
minister with or immediately following 6h as needed (Maximum: 1,000 mg).

Canadian trade name Non-Crushable Drug High Alert drug


178 canagliflozin
IV: (Calcium Gluconate): ADULTS, EL- tions, altered taste). Calcium carbon-
DERLY: (Mild): 1–2 g over 2 hrs; (Moder- ate: Milk-alkali syndrome (headache,
ate to severe, asymptomatic): 4 g over 4 decreased appetite, nausea, vomiting,
C hrs; (Severe, symptomatic): 1–2 g over unusual fatigue). Rare: Urinary urgency,
10 min; may repeat q60min until symp- painful urination.
toms resolve. CHILDREN: 200–500 mg/
kg/day as a continuous infusion or in 4 ADVERSE EFFECTS/TOXIC
divided doses. (Maximum: 1,000 mg). REACTIONS
NEONATES: 200 mg/kg q6–12h or 400 Hypercalcemia: Early signs: Consti-
mg/kg/day as a continuous infusion. pation, headache, dry mouth, increased
thirst, irritability, decreased appetite, me-
Antacid tallic taste, fatigue, weakness, depression.
PO: (Calcium Carbonate): ADULTS, Later signs: Confusion, drowsiness, hy-
ELDERLY: 1–4 tabs as needed. Maxi- pertension, photosensitivity, arrhythmias,
mum: 8,000 mg/day. CHILDREN 12 YRS nausea, vomiting, painful urination.
AND OLDER: 500–3,000 mg for up to 2
wks. Maximum: 7,500 mg/day. CHIL- NURSING CONSIDERATIONS
DREN 6–11 YRS: 750–800 mg/day for up
BASELINE ASSESSMENT
to 2 wks. Maximum: 3,000 mg/day.
CHILDREN 2–5 YRS: 375–400 mg/day for Assess B/P, ECG and cardiac rhythm,
up to 2 wks. Maximum: 1,500 mg/day. renal function, serum magnesium, phos-
phate, calcium, ionized calcium.
Cardiac Arrest
INTERVENTION/EVALUATION
IV: (Calcium Chloride): ADULTS, EL-
DERLY: 500–1,000 mg over 2–5 min. Monitor serum BMP, calcium, ionized
May repeat as necessary. CHILDREN, calcium, magnesium, phosphate; B/P,
NEONATES: 20 mg/kg. May repeat in 10 cardiac rhythm, renal function. Monitor
min if necessary. If effective, consider for signs of hypercalcemia.
IV infusion of 20–50 mg/kg/hr. Maxi- PATIENT/FAMILY TEACHING
mum: 2,000 mg/dose.
• Do not take within 1–2 hrs of other oral
Supplement medications, fiber-containing foods. •
PO: (Calcium Carbonate): ADULTS, EL- Avoid excessive use of alcohol, tobacco,
DERLY: 500 mg–4 g/day in 1–3 divided caffeine.
doses. CHILDREN OLDER THAN 4 YRS: 750
mg 3 times/day. CHILDREN 2–4 YRS: 750
mg 2 times/day. (Calcium Citrate): canagliflozin
ADULTS, ELDERLY: 0.5–2 g 2–4 times/day.
CHILDREN: 45–65 mg/kg/day in 4 divided kan-a-gli-floe-zin
doses. (Invokana)
Dosage in Renal/Hepatic Impairment j BLACK BOX ALERT jMay in-
crease risk of lower limb amputations,
No dose adjustment. including the toe, midfoot, and leg.
Some pts had multiple amputations,
SIDE EFFECTS including both legs. Monitor for new
Frequent: PO: Chalky taste. Paren- pain, tenderness, ulcers of lower legs.
teral: Pain, rash, redness, burning at
injection site; flushing, nausea, vomiting,
FIXED-COMBINATION(S)
diaphoresis, hypotension. Occasional: Invokamet: canagliflozin/metFOR-
PO: Mild constipation, fecal impaction, MIN (an antidiabetic): 50 mg/500 mg,
peripheral edema, metabolic alkalosis 50 mg/1,000 mg, 150 mg/500 mg, 150
(muscle pain, restlessness, slow respira- mg/1,000 mg.

underlined – top prescribed drug


canagliflozin 179
uCLASSIFICATION for adverse reactions (e.g., hypotension,
PHARMACOTHERAPEUTIC: Sodium- syncope, dehydration).
glucose co-transporter 2 (SGLT2) INTERACTIONS
inhibitor. CLINICAL: Antidiabetic. C
DRUG: CarBAMazepine, ­fosphenytoin,
PHENobarbital, phenytoin may de-
USES crease concentration/effect. May increase
Adjunctive treatment to diet and exercise hypotensive effect of loop ­diuretics
to improve glycemic control in pts with (e.g., bumetanide, furosemide). In-
type 2 diabetes mellitus; risk reduction sulin may increase risk of hypoglycemia.
of major cardiovascular events (cardio- May increase concentration/effects of di-
vascular death, nonfatal MI, and nonfatal goxin. HERBAL: St. John’s wort may de-
stroke) in adults with type 2 diabetes and crease concentration/effect. FOOD: None
established CV disease. known. LAB VALUES: May increase se-
rum low-density lipoprotein-cholesterol
PRECAUTIONS (LDL-C), Hgb, creatinine, magnesium,
Contraindications: History of hypersensi- phosphate, potassium. May decrease glo-
tivity to canagliflozin, other SGLT2 inhibi- merular filtration rate.
tors, severe renal impairment, end-stage
renal disease, dialysis. Cautions: Not rec- AVAILABILITY (Rx)
ommended in type 1 diabetes, diabetic Tablets: 100 mg, 300 mg.
ketoacidosis. Concurrent use of diuret-
ics, ACE inhibitors, angiotensin receptor ADMINISTRATION/HANDLING
blockers (ARB), other hypoglycemic or PO
nephrotoxic medications; mild to mod- • Give before first meal of the day.
erate renal impairment, hypovolemia
(dehydration/anemia), elderly, episodic INDICATIONS/ROUTES/DOSAGE
hypotension, hyperkalemia, genital my- Type 2 Diabetes Mellitus
cotic infection. PO: ADULTS/ELDERLY: 100 mg daily be-
ACTION fore first meal. May increase to 300 mg
Increases excretion of urinary glucose by daily if glomerular filtration rate (GFR)
inhibiting reabsorption of filtered glucose greater than 60 mL/min.
in kidney. Inhibits SGLT2 in proximal re- Dosage in Renal Impairment
nal tubule. Therapeutic Effect: Lowers GFR 45–60 mL/min: 100 mg daily
serum glucose levels. (maximum). GFR less than 45 mL/
PHARMACOKINETICS min: Permanently discontinue.
Readily absorbed following PO adminis-
Dosage in Hepatic Impairment
tration. Metabolized in liver. Peak plasma
concentration: 1–2 hrs. Protein binding: No dose adjustment.
99%. Excreted in feces (42%), urine
(33%). Half-life: 11–13 hrs. SIDE EFFECTS
Occasional (5%): Increased urination. Rare
LIFESPAN CONSIDERATIONS (3%–2%): Thirst, nausea, constipation.
Pregnancy/Lactation: Unknown if
distributed in breast milk. Must either ADVERSE EFFECTS/TOXIC
discontinue drug or discontinue breast- REACTIONS
feeding. Children: Safety and efficacy Symptomatic hypotension (postural
not established in pts younger than 18 dizziness, orthostatic hypotension, syn-
yrs. Elderly: May have increased risk cope) may occur. Genital mycotic (yeast)

Canadian trade name Non-Crushable Drug High Alert drug


180 candesartan
infections reported in 10% of pts. Hy- any palpitations or muscle weakness.
poglycemic events reported in 1.5% of • Treatment may cause loss of limbs;
pts (5% in elderly). Concomitant use of immediately report new leg ulcers, pain,
C hypoglycemic medications may increase tenderness.
hypoglycemic risk. Hypersensitivity reac-
tions, including angioedema, urticaria,
rash, pruritus, erythema, occurred in
3%–4% of pts. May cause hyperkalemia.
candesartan
May increase risk of ketoacidosis. kan-de-sar-tan
NURSING CONSIDERATIONS (Atacand)
j BLACK BOX ALERT jMay
BASELINE ASSESSMENT cause fetal injury, mortality. Dis-
continue as soon as possible once
Assess hydration status. Obtain BMP, cap- pregnancy is detected.
illary blood glucose, hemoglobin A1c,
LDL-C, digoxin level (if applicable). As- FIXED-COMBINATION(S)
sess pt’s understanding of diabetes man- Atacand HCT: candesartan/hydro-
agement, routine blood glucose moni- CHLOROthiazide (a diuretic): 16
toring. Receive full medication history, mg/12.5 mg, 32 mg/12.5 mg.
including minerals, herbal products.
Question history of co-morbidities, esp. uCLASSIFICATION
renal or hepatic impairment. PHARMACOTHERAPEUTIC: Angio-
INTERVENTION/EVALUATION tensin II receptor blocker. CLINI-
Monitor serum potassium, cholesterol; cap- CAL: Antihypertensive.
illary blood glucose, hepatic/renal function
tests. Assess for hypoglycemia, hypersensi- USES
tivity reaction. Monitor for signs of hyper-
kalemia. Screen for glucose-altering con- Treatment of hypertension alone or in
ditions: fever, increased activity or stress, combination with other antihyperten-
surgical procedures. Obtain dietary consult sives, HF: NYHA class II–IV.
for nutritional education. Encourage PO in- PRECAUTIONS
take. Diligently monitor for new leg ulcers,
sores, pain; wound may lead to amputation. Contraindications: Hypersensitivity to can-
desartan. Concomitant use with aliskiren
PATIENT/FAMILY TEACHING in pts with diabetes mellitus. Cautions: Sig-
• Diabetes mellitus requires lifelong nificant aortic/mitral stenosis, renal/hepatic
control. • Diet and exercise are prin- impairment, unstented (unilateral/bilat-
cipal parts of treatment; do not skip or eral) renal artery stenosis, HF (may induce
delay meals. • Test blood sugar regu- hypotension when treatment initiated).
larly. • When taking combination drug
therapy or when glucose demands are ACTION
altered (fever, infection, trauma, stress), Blocks vasoconstriction, aldosterone-se-
have low blood sugar treatment avail- creting effects of angiotensin II, inhibiting
able (glucagon, oral dextrose). • Re- binding of angiotensin II to AT1 receptors.
port suspected pregnancy or plans of Therapeutic Effect: Produces vasodila-
breastfeeding. • Monitor daily calorie tion; decreases peripheral resistance, B/P.
intake. • Go from lying to standing
slowly to prevent dizziness. • Genital PHARMACOKINETICS
itching may indicate yeast infection. Route Onset Peak Duration
• Therapy may increase risk for dehy- PO 2–3 hrs 6–8 hrs Greater than
dration/low blood pressure. • Report 24 hrs

underlined – top prescribed drug


candesartan 181
Rapidly, completely absorbed. Protein HF
binding: greater than 99%. Undergoes PO: ADULTS, ELDERLY: Initially, 4–8 mg
minor hepatic metabolism to inactive once daily. May double dose at approxi-
metabolite. Excreted unchanged in urine mately 2-wk intervals up to a target dose C
and in feces through biliary system. Not re- of 32 mg/day.
moved by hemodialysis. Half-life: 9 hrs.
Dosage in Renal/Hepatic Impairment
LIFESPAN CONSIDERATIONS Mild to moderate impairment: No
Pregnancy/Lactation: Unknown if dose adjustment. Severe impair-
distributed in breast milk. May cause ment: Use caution.
fetal/neonatal morbidity/mortality. Chil- SIDE EFFECTS
dren: Safety and efficacy not established
Occasional (6%–3%): Upper respiratory
in pts younger than 1 yr. Elderly: No tract infection, dizziness, back/leg pain.
age-related precautions noted. Rare (2%–1%): Pharyngitis, rhinitis, head-
INTERACTIONS ache, fatigue, diarrhea, nausea, dry cough,
DRUG: May increase risk of lithium toxic- peripheral edema.
ity. NSAIDs (e.g., ibuprofen, ketorolac, ADVERSE EFFECTS/TOXIC
naproxen) may decrease effects. Aliski- REACTIONS
ren may increase hyperkalemic effect. May Overdosage may manifest as hypotension,
increase adverse/toxicity of ACE inhibitors tachycardia. Bradycardia occurs less of-
(e.g., benazepril, lisinopril). HERBAL: ten. May increase risk of renal failure,
Herbals with hypertensive properties hyperkalemia.
(e.g., licorice, yohimbe) or hypotensive
properties (e.g., garlic, ginger, ginkgo NURSING CONSIDERATIONS
biloba) may alter effects. FOOD: None
known. LAB VALUES: May increase serum BASELINE ASSESSMENT
BUN, alkaline phosphatase, bilirubin, creati- Obtain B/P, apical pulse immediately before
nine, ALT, AST. May decrease Hgb, Hct. each dose in addition to regular monitoring
(be alert to fluctuations). Obtain pregnancy
AVAILABILITY (Rx) test in female pts of reproductive potential.
Tablets: 4 mg, 8 mg, 16 mg, 32 mg. Assess medication history (esp. diuretic).
Question for history of hepatic/renal im-
ADMINISTRATION/HANDLING pairment, renal artery stenosis. Obtain se-
PO rum BUN, creatinine, LFT; Hgb, Hct.
• Give without regard to food.
INTERVENTION/EVALUATION
INDICATIONS/ROUTES/DOSAGE Maintain hydration (offer fluids fre-
Hypertension quently). Assess for evidence of upper
Note: Antihypertensive effect usually seen respiratory infection. Assist with ambula-
in 2 wks. Maximum effect within 4–6 wks. tion if dizziness occurs. Monitor electro-
PO: ADULTS, ELDERLY: Initially, 8–16 mg lytes, renal function, urinalysis. Assess
once daily. Titrate to response. Range: 8–32 B/P for hypertension/hypotension. If ex-
mg/day in 1–2 divided doses. CHILDREN cessive reduction in B/P occurs, place pt
6–16 YRS, MORE THAN 50 KG: Initially, in supine position, feet slightly elevated.
8–16 mg/day in 1–2 divided doses. Range: PATIENT/FAMILY TEACHING
4–32 mg. Maximum: 32 mg/day. 50 KG OR
LESS: Initially, 4–8 mg in 1–2 divided doses.
• Hypertension requires lifelong control. •
Range: 2–16 mg/day. Maximum: 32 mg/ Inform female pts regarding potential for
day. CHILDREN 1–5 YRS: Initially, 0.2 mg/kg/ fetal injury, mortality with second- and third-
day in 1–2 divided doses. Range: 0.05–0.4 trimester exposure to candesartan. • Re-
mg/kg/day. Maximum: 0.4 mg/kg/day. port suspected pregnancy. • Avoid tasks

Canadian trade name Non-Crushable Drug High Alert drug


182 capecitabine
that require alertness, motor skills until re- with DNA synthesis, RNA processing, pro-
sponse to drug is established. • Report tein synthesis.
any sign of infection (sore throat, fever).
C • Do not stop taking medication. • Cau- PHARMACOKINETICS
tion against exercising during hot weather Readily absorbed from GI tract. Protein
(risk of dehydration, hypotension). binding: less than 60%. Metabolized in
liver. Primarily excreted in urine. Half-
life: 45 min.
capecitabine LIFESPAN CONSIDERATIONS
kap-e-sye-ta-bine Pregnancy/Lactation: May cause fetal
(Xeloda) harm. Unknown if distributed in breast
j BLACK BOX ALERT jMay milk. Children: Safety and efficacy not
increase anticoagulant effect of established in pts younger than 18 yrs.
warfarin. Fatal hemorrhagic events Elderly: May be more sensitive to GI
have occurred. side effects.
Do not confuse capecitabine
with decitabine or emtricit- INTERACTIONS
abine, or Xeloda with Xenical. DRUG: May increase concentration, tox-
icity of warfarin, phenytoin. Myelosup-
uCLASSIFICATION
pression may be enhanced when given
PHARMACOTHERAPEUTIC: Antime- concurrently with bone marrow depres-
tabolite. CLINICAL: Antineoplastic. sants. Live virus vaccines may potenti-
ate virus replication, increase vaccine side
USES effects, decrease pt’s antibody response
Treatment of metastatic breast cancer to vaccine. May decrease therapeutic ef-
as monotherapy or in combination with fect of BCG (intravesical). Allopuri-
docetaxel after failure of prior anthracycline- nol may decrease concentration/effect.
HERBAL: Echinacea may decrease level/
containing regimen. Treatment of metastatic
colorectal cancer. Adjuvant (postsurgical) effects. FOOD: None known. LAB VAL-
UES: May increase serum alkaline phos-
treatment of Dukes C colon cancer. OFF-
LABEL: Gastric cancer, pancreatic cancer,
phatase, bilirubin, ALT, AST. May decrease
esophageal cancer, ovarian cancer, neuro- Hgb, Hct, WBC. May increase PT/INR.
endocrine tumors, hepatobiliary cancer. AVAILABILITY (Rx)
PRECAUTIONS Tablets: 150 mg, 500 mg.
Contraindications: Severe renal impair- ADMINISTRATION/HANDLING
ment (CrCl less than 30 mL/min), dihy-
dropyrimidine dehydrogenase (DPD) • Give within 30 min after meals with wa-
deficiency, hypersensitivity to capecitabine, ter. • Administer whole; do not cut, crush.
5-fluorouracil (5-FU). Cautions: Existing INDICATIONS/ROUTES/DOSAGE
bone marrow depression, hepatic impair-
ment, mild to moderate renal impairment, Metastatic Breast Cancer (as
previous cytotoxic therapy/radiation ther- Monotherapy or in Combination with
apy, elderly (60 yrs of age or older). Docetaxel), Metastatic Colorectal Cancer,
Adjuvant (Postsurgery) Treatment of
ACTION Dukes C Colon Cancer
Enzymatically converted to 5-fluorouracil PO: ADULTS, ELDERLY: Initially, 2,500 mg/
(5-FU). Inhibits enzymes necessary for m2/day in 2 equally divided doses approxi-
synthesis of essential cellular compo- mately q12h apart for 2 wks. Follow with
nents. Therapeutic Effect: Interferes a 1-wk rest period; given in 3-wk cycles.

underlined – top prescribed drug


captopril 183
Dosage in Renal Impairment PATIENT/FAMILY TEACHING
CrCl 51–80 mL/min: No adjustment. • Report nausea, vomiting, diarrhea, hand-
CrCl 30–50 mL/min: 75% of normal and-foot syndrome, stomatitis. • Do not
dose. CrCl less than 30 mL/min: Con- have immunizations without physician’s ap- C
traindicated. proval (drug lowers body’s resistance).
Dosage in Hepatic Impairment
• Avoid contact with those who have
No dose adjustment at start of therapy; inter- recently received live virus vaccine.
rupt therapy for Grade 3 or 4 hyperbilirubi- • Promptly report fever higher than
nemia until bilirubin is 3 times ULN or less. 100.5°F, sore throat, signs of local infection,
unusual bruising/bleeding from any site.
SIDE EFFECTS
Frequent (55%–25%): Diarrhea, nausea,
vomiting, stomatitis, fatigue, anorexia, derma-
captopril
titis. Occasional (24%–10%): Constipation, kap-toe-pril
dyspepsia, headache, dizziness, insomnia,
edema, myalgia, pyrexia, dehydration,
j BLACK BOX ALERT jMay
cause injury/death to developing
dyspnea, back pain. Rare (less than 10%): fetus. Discontinue as soon as pos-
Mood changes, depression, sore throat, epi- sible once pregnancy is detected.
staxis, cough, visual abnormalities. Do not confuse captopril with
calcitriol, Capitrol, carvedilol,
ADVERSE EFFECTS/TOXIC enalapril, fosinopril, lisinopril,
REACTIONS Monopril, or quinapril.
Serious reactions include myelosuppres-
sion (neutropenia, thrombocytopenia, FIXED-COMBINATION(S)
anemia), cardiovascular toxicity (angina, Capozide: captopril/hydroCHLORO-
cardiomyopathy, DVT), respiratory tox- thiazide (a diuretic): 25 mg/15 mg, 25
icity (dyspnea, epistaxis, pneumonia), mg/25 mg, 50 mg/15 mg, 50 mg/25 mg.
lymphedema. Palmar-plantar erythro-
dysesthesia syndrome (PPES), present- uCLASSIFICATION
ing as redness, swelling, numbness, skin PHARMACOTHERAPEUTIC: Angio-
sloughing of hands and feet, may occur. tensin-converting enzyme (ACE) in-
hibitor. CLINICAL: Antihypertensive,
NURSING CONSIDERATIONS vasodilator.
BASELINE ASSESSMENT
Assess sensitivity to capecitabine or USES
5-fluorouracil. Obtain baseline Hgb, Hct, Treatment of hypertension, HF, diabetic
serum chemistries, renal function. nephropathy, post-MI to improve survival
INTERVENTION/EVALUATION in pts with left ventricular dysfunction.
Monitor for severe diarrhea, nausea, PRECAUTIONS
vomiting; if dehydration occurs, fluid and Contraindications: Hypersensitivity to cap-
electrolyte replacement therapy should topril. History of angioedema from previous
be initiated. Assess hands/feet for PPES. treatment with ACE inhibitors, concomitant
Monitor CBC for evidence of bone mar- use with aliskiren in pts with diabetes mel-
row depression. Monitor renal/hepatic litus. Coadministration with or within 36
function. Monitor for blood dyscrasias hrs of switching to or from a neprilysin
(fever, sore throat, signs of local infec- inhibitor (e.g., sacubitril). Cautions: Renal
tion, unusual bruising/bleeding from any impairment; hypertrophic cardiomyopathy
site), symptoms of anemia (excessive fa- with outflow obstruction before, during, or
tigue, weakness). immediately after major surgery. Unstented
Canadian trade name Non-Crushable Drug High Alert drug
184 captopril
unilateral/bilateral renal artery stenosis. AVAILABILITY (Rx)
Concomitant use of potassium-sparing di- Tablets: 12.5 mg, 25 mg, 50 mg, 100 mg.
uretics, potassium supplements.
C ADMINISTRATION/HANDLING
ACTION PO
Suppresses renin-angiotensin-aldoste- • Administer 1 hr before or 2 hrs after
rone system (prevents conversion of an- meals for maximum absorption (food
giotensin I to angiotensin II, a potent vaso- may decrease drug absorption). • Tab-
constrictor; may inhibit angiotensin II at lets may be crushed.
local vascular and renal sites). Decreases
plasma angiotensin II, increases plasma INDICATIONS/ROUTES/DOSAGE
renin activity, decreases aldosterone se- Hypertension
cretion. Therapeutic Effect: Lowers BP. PO: ADULTS, ELDERLY: Initially, 12.5–25
Improves HF, diabetic neuropathy. mg 2–3 times/day. May increase by
12.5–25 mg/dose at 1–2-wk intervals up
PHARMACOKINETICS to 50 mg 3 times/day. Add diuretic before
Route Onset Peak Duration further increase in dose. Maximum: 450
PO 0.25 hr 0.5–1.5 hrs Dose-related mg/day in 3 divided doses. CHILDREN, ADO-
LESCENTS: 0.3–0.5 mg 3 times/day. Max-
Rapidly, well absorbed from GI tract (ab- imum: 6 mg/kg/day in 3 divided doses.
sorption decreased in presence of food). INFANTS: 0.15–0.3 mg/kg/dose. May
Protein binding: 25%–30%. Metabolized in titrate up to maximum of 6 mg/kg/day in 3
liver. Primarily excreted in urine. Removed divided doses. Usual range: 2.5–6 mg/kg/
by hemodialysis. Half-life: Less than 3 day in 3 divided doses. NEONATES: 0.01–
hrs (increased in renal impairment). 0.1 mg/kg/dose q8–24h. Maximum: 0.5
mg/kg/dose q6–24h.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses pla- HF
centa; distributed in breast milk. May PO: ADULTS, ELDERLY: Initially, 6.25–25
cause fetal/neonatal mortality/morbidity. mg 3 times/day. Target dose: 50 mg 3
Children: Safety and efficacy not estab- times/day.
lished. Elderly: May be more sensitive
Post-MI
to hypotensive effects.
PO: ADULTS, ELDERLY: Initially, 6.25 mg.
INTERACTIONS If tolerated, then 12.5 mg 3 times/day. In-
crease to 25 mg 3 times/day over several
DRUG: Aliskiren may increase hyperkale-
days, up to target dose of 50 mg 3 times/
mic effect. May increase potential for allergic
day over several wks.
reactions to allopurinol. Angiotensin II
receptor blockers (ARBs) (e.g., losar- Diabetic Nephropathy
tan, valsartan) may increase adverse ef- PO: ADULTS, ELDERLY: 25 mg 3 times/day.
fects. May increase adverse effects of lith-
ium, sacubitril. HERBAL: Herbals with Dosage in Renal Impairment
hypertensive properties (e.g., licorice, CrCl 10–50 mL/min: 75% of nor-
yohimbe) or hypotensive properties mal dosage. CrCl less than 10 mL/
(e.g., garlic, ginger, ginkgo biloba) min: 50% of normal dosage.
may alter effects. FOOD: Licorice may cause Dosage in Hepatic Impairment
sodium and water retention, hypokalemia. No dose adjustment.
LAB VALUES: May increase serum BUN,
alkaline phosphatase, bilirubin, creatinine, SIDE EFFECTS
potassium, ALT, AST. May decrease serum Frequent (7%–4%): Rash. Occasional
sodium. May cause positive ANA titer. (4%–2%): Pruritus, dysgeusia. Rare (less

underlined – top prescribed drug


carBAMazepine 185
than 2%): Headache, cough, insomnia, diarrhea, excessive perspiration, dehydra-
dizziness, fatigue, paresthesia, malaise, tion, persistent cough, sore throat, fever
nausea, diarrhea or constipation, dry occur. • Inform physician if pregnant or
mouth, tachycardia. planning to become pregnant. • Rise C
slowly from sitting/lying position.
ADVERSE EFFECTS/TOXIC
REACTIONS
Hypotension (“first-dose syncope”) may
occur in pts with HF and in those who are carBAMazepine
severely sodium/volume depleted. Angio-
edema, hyperkalemia occur rarely. Agran- kar-ba-maz-e-peen
ulocytosis, neutropenia noted in those with (Carbatrol, Epitol, Equetro,
collagen vascular disease (scleroderma, ­TEGretol, TEGretol XR)
systemic lupus erythematosus), renal im- j BLACK BOX ALERT jPoten-
pairment. Nephrotic syndrome noted in tially fatal aplastic anemia, agranu-
those with history of renal disease. locytosis reported. Potentially fatal,
severe dermatologic reactions (e.g.,
NURSING CONSIDERATIONS Stevens-Johnson syndrome, toxic
epidermal necrolysis) may occur.
BASELINE ASSESSMENT Risk increased in pts with the
variant HLA-β* 1502 allele, almost
Obtain B/P immediately before each dose exclusively in pts of Asian ancestry.
in addition to regular monitoring (be Do not confuse carBAMazepine
alert to fluctuations). If hypotension oc- with OXcarbazepine, eslicar-
curs, place pt in supine position with legs bazepine, or TEGretol with
elevated. In pts with prior renal disease Mebaral, Toprol XL, Toradol, or
or receiving dosages greater than 150 TRENtal.
mg/day, test urine for protein by dipstick
method with first urine of day before uCLASSIFICATION
therapy begins and periodically thereaf- PHARMACOTHERAPEUTIC: Imino-
ter. In pts with renal impairment, autoim- stilbene derivative. CLINICAL: Anti-
mune disease, or taking drugs that affect convulsant.
leukocytes or immune response, obtain
CBC before beginning therapy, q2wks for
3 mos, then periodically thereafter. USES
INTERVENTION/EVALUATION
Carbatrol, Epitol, TEGretol, TEGre-
tol XR: Treatment of partial seizures
Assess skin for rash, pruritus. Assist with with complex symptomatology, general-
ambulation if dizziness occurs. Monitor ized tonic-clonic seizures, mixed seizure
urinalysis for proteinuria. Monitor serum patterns, pain relief of trigeminal, glos-
potassium levels in pts on concurrent di- sopharyngeal neuralgia. Equetro: Acute
uretic therapy. Monitor B/P, serum BUN, manic and mixed episodes associated
creatinine, CBC. Discontinue medication, with bipolar disorder. OFF-LABEL: Neuro-
contact physician if angioedema occurs. pathic pain in critically ill pts.
PATIENT/FAMILY TEACHING
• Full therapeutic effect of B/P reduction PRECAUTIONS
may take several wks. • Skipping doses Contraindications: Concomitant use or
or voluntarily discontinuing drug may within 14 days of use of MAOIs, myelo-
produce severe rebound hyperten- suppression. Concomitant use of dela-
sion. • Limit alcohol intake. • Imme- virdine or other NNRT inhibitors that are
diately report if swelling of face, lips, substrates of CYP3A4. Hypersensitivity
or tongue, difficulty breathing, vomiting, to carBAMazepine, tricyclic antidepres-
Canadian trade name Non-Crushable Drug High Alert drug
186 carBAMazepine
sants. Cautions: High risk of suicide, g­lucose, alkaline phosphatase, bilirubin,
increased IOP, hepatic or renal impair- ALT, AST, cholesterol, HDL, triglycerides.
ment, history of cardiac impairment, ECG May decrease serum calcium, thyroid hor-
C abnormalities, elderly. mone (T3, T4 index) levels. Therapeutic
serum level: 4–12 mcg/mL; toxic se-
ACTION rum level: greater than 12 mcg/mL.
Decreases sodium ion influx into neuronal
membranes (may depress activity in thala- AVAILABILITY (Rx)
mus, decreasing synaptic transmission or Suspension, Oral: (TEGretol): 100 mg/5
decreasing temporal stimulation, leading mL. Tablets: (Epitol, TEGretol): 200 mg.
to neural discharge). Therapeutic Ef- Tablets: (Chewable [TEGretol]): 100 mg.
fect: Produces anticonvulsant effect. Capsules: (Extended-Release [Car-
batrol, Equetro]): 100 mg, 200 mg, 300
PHARMACOKINETICS mg. Tablets: (Extended-Release [TEGretol
Slowly, completely absorbed from GI tract. XR]): 100 mg, 200 mg, 400 mg.
Protein binding: 75%–90%. Metabolized
in liver. Primarily excreted in urine. Not re- ADMINISTRATION/HANDLING
moved by hemodialysis. Half-life: 25–65 PO
hrs (decreased with chronic use). • Store oral suspension, tablets at room
temperature. • Give with meals to re-
LIFESPAN CONSIDERATIONS duce GI distress. • May give extended-
Pregnancy/Lactation: Crosses placenta; release capsules without regard to
distributed in breast milk. Accumulates in food. • Extended-release tablets should
fetal tissue. Children: Behavioral changes be given with meals. • Shake oral sus-
more likely to occur. Elderly: More sus- pension well. Do not administer simulta-
ceptible to confusion, agitation, AV block, neously with other liquid medicine. • Do
bradycardia, syndrome of inappropriate not crush or open extended-release cap-
antidiuretic hormone (SIADH). sules or tablets. • Extended-release cap-
sules may be opened and sprinkled over
INTERACTIONS food (e.g., applesauce).
DRUG: CYP3A4 inhibitors (e.g., ci-
metidine, clarithromycin, azole INDICATIONS/ROUTES/DOSAGE
antifungals, protease inhibitors) b ALERT c Suspension must be given
may increase concentration. CYP3A4 on a 3–4 times/day schedule; tablets on a
inducers (e.g., rifAMPin, phe- 2–4 times/day schedule; extended-re-
nytoin) may decrease concentration/ lease capsules 2 times/day. (Carnexiv):
effects. May decrease concentration/ 70% of total oral dose given as four 30-
effects of hormonal contraceptives, min infusions separated by 6 hrs.
warfarin, traZODone. May decrease
concentration/effects of abemaci- Seizure Control
clib, apixaban, axitinib, bosutinib, PO: ADULTS, ELDERLY, CHILDREN OLDER
brigatinib, dronedarone, nifedip- THAN 12 YRS: Initially, 200 mg twice daily
ine, ranolazine, regorafenib, vora- (tablet or extended-release or in 4 divided
paxar, voriconazole. May decrease doses as suspension). May increase dosage
therapeutic effect of BCG (intravesical). by 200 mg/day at wkly intervals. Usual dose:
HERBAL: Gotu kola, kava kava, vale- 800–1,200 mg/day in 2–4 divided doses.
rian may increase CNS depression. St. Maximum: ADULTS, ELDERLY: 1,600 mg/
John’s wort may decrease concentra- day; CHILDREN OLDER THAN 15 YRS: 1,200
tion/effect. FOOD: Grapefruit products mg/day; CHILDREN 13–15 YRS: 1,000 mg/
may increase absorption, concentration. day. CHILDREN 6–12 YRS: Initially, 100 mg
LAB VALUES: May increase serum BUN, twice daily (tablets) or 4 times/day (oral

underlined – top prescribed drug


carBAMazepine 187
suspension). May increase by 100 mg/day cytosis, eosinophilia), cardiovascular
at wkly intervals. Usual dose: 400–800 disturbances (HF, hypotension/hyperten-
mg/day. Maximum: 1,000 mg/day. sion, thrombophlebitis, arrhythmias),
CHILDREN YOUNGER THAN 6 YRS: Initially, dermatologic effects (rash, urticaria, C
10–20 mg/kg/day 2–3 times/day (tablets) pruritus, photosensitivity). Abrupt with-
or 4 times/day (suspension). May increase drawal may precipitate status epilepticus.
at wkly intervals until optimal response
and therapeutic levels are achieved. Maxi- NURSING CONSIDERATIONS
mum: 35 mg/kg/day. BASELINE ASSESSMENT
Trigeminal, Glossopharyngeal Neuralgia, CBC, serum iron determination, urinaly-
Diabetic Neuropathy sis, BUN should be performed before
PO: ADULTS, ELDERLY: Initially, 200 mg/ therapy begins and periodically during
day as single dose (extended-release), or therapy. Seizures: Review history of
100 mg in 2 divided doses (immediate- seizure disorder (intensity, frequency,
release), or 50 mg 4 times/day (oral duration, level of consciousness [LOC]).
suspension). May increase by 200 mg/ Initiate seizure precautions. Neuralgia:
day as needed. Give extended release in Assess facial pain, stimuli that may cause
2 divided doses if total daily dose exceeds facial pain. Bipolar: Assess mental sta-
200 mg. Usual dose: 400–800 mg daily. tus, cognitive abilities.
Maximum: 1,200 mg/day. INTERVENTION/EVALUATION
Bipolar Disorder Seizures: Observe frequently for recur-
PO: ADULTS, ELDERLY: (Equetro):Initially, rence of seizure activity. Monitor therapeutic
400 mg/day in 2 divided doses. May ad- levels. Assess for clinical improvement (de-
just dose in 200-mg increments. Maxi- crease in intensity, frequency of seizures).
mum: 1,600 mg/day in divided doses. Assess for clinical evidence of early toxic-
ity (fever, sore throat, mouth ulcerations,
Dosage in Renal Impairment unusual bruising/bleeding, joint pain).
CrCl less than 10 mL/min: 75% of Neuralgia: Avoid triggering tic douloureux
normal dose. HD: 75% of normal dose. (draft, talking, washing face, jarring bed,
CRRT: 75% of normal dose. hot/warm/cold food or liquids). Bipolar:
Monitor for suicidal ideation, behavioral
Dosage in Hepatic Impairment changes. Observe for excessive sedation.
Use caution. Therapeutic serum level: 4–12 mcg/
mL; toxic serum level: greater than
SIDE EFFECTS 12 mcg/mL.
Frequent (greater than 10%): Vertigo, som-
PATIENT/FAMILY TEACHING
nolence, ataxia, fatigue, leukopenia, rash,
urticaria, nausea, vomiting. Occasional • Do not abruptly discontinue medication
(10%–1%): Headache, diplopia, blurred vi- after long-term use (may precipitate sei-
sion, thrombocytopenia, dry mouth, edema, zures). • Strict maintenance of therapy is
fluid retention, increased weight. Rare (less essential for seizure control. • Avoid tasks
than 1%): Tremors, visual disturbances, that require alertness, motor skills until re-
lymphadenopathy, jaundice, involuntary sponse to drug is established. • Report
muscle movements, nystagmus, dermatitis. visual disturbances. • Blood tests should
be repeated frequently during first 3 mos of
ADVERSE EFFECTS/TOXIC therapy and at monthly intervals thereafter
REACTIONS for 2–3 yrs. • Do not take oral suspen-
Toxic reactions appear as blood dyscra- sion simultaneously with other liquid medi-
sias (aplastic anemia, agranulocytosis, cine. • Do not ingest grapefruit prod-
thrombocytopenia, leukopenia, leuko- ucts. • Report serious skin reactions.
Canadian trade name Non-Crushable Drug High Alert drug
188 carbidopa/levodopa
cholinergic activity. Carbidopa prevents
carbidopa/levodopa peripheral breakdown of levodopa, mak-
ing more levodopa available for transport
C kar-bi-doe-pa/lee-voe-doe-pa into brain. Therapeutic Effect: Treats
(Apo-Levocarb , Duopa, Rytary, symptoms associated with Parkinson’s
Sinemet, Sinemet CR) disease.
Do not confuse Sinemet with
Serevent. PHARMACOKINETICS
Rapidly and completely absorbed from
FIXED-COMBINATION(S) GI tract. Widely distributed. Excreted pri-
Stalevo: carbidopa/levodopa/enta- marily in urine. Levodopa is converted to
capone (antiparkinson agent): 12.5 DOPamine. Excreted primarily in urine.
mg/50 mg/200 mg, 18.75 mg/75 Half-life: 1–2 hrs (carbidopa); 1–3
mg/200 mg, 25 mg/100 mg/200 hrs (levodopa).
mg, 31.25 mg/125 mg/200 mg, 37.5
mg/150 mg/200 mg, 50 mg/200 LIFESPAN CONSIDERATIONS
mg/200 mg. Pregnancy/Lactation: Unknown if
drug crosses placenta or is distributed
uCLASSIFICATION
in breast milk. May inhibit lactation.
PHARMACOTHERAPEUTIC: DO- Breastfeeding not recommended. Chil-
Pamine precursor. Decarboxylase dren: Safety and efficacy not established
inhibitor. CLINICAL: Antiparkinson in pts younger than 18 yrs. Elderly: More
agent. sensitive to effects of levodopa. Anxiety,
confusion, nervousness more common
when receiving anticholinergics.
USES
Treatment of Parkinson’s disease, post- INTERACTIONS
encephalitic parkinsonism, symptomatic DRUG: Antipsychotics, pyridoxine may
parkinsonism following CNS injury by decrease therapeutic effect. May increase
carbon monoxide poisoning, manganese adverse effects of MAOIs (e.g., phen-
intoxication. Duopa: Treatment of mo- elzine, selegiline). HERBAL: None sig-
tor fluctuations in advanced Parkinson’s nificant. FOOD: High-protein diets may
disease.  OFF-LABEL: Restless legs syn- cause decreased or erratic response to
drome. levodopa. LAB VALUES: May increase
serum BUN, LDH, alkaline phosphatase,
PRECAUTIONS
bilirubin, ALT, AST. May decrease Hgb, Hct,
Contraindications: Hypersensitivity to car- WBC.
bidopa/levodopa. Concurrent use with
MAOIs or use within 14 days. (Tablets AVAILABILITY (Rx)
only): Narrow-angle glaucoma. Cau- Enteral Suspension: (Duopa): 100-mL
tions: History of MI, arrhythmias, bronchial cassette containing 4.63 mg carbidopa
asthma, emphysema, severe cardiac, pul- and 20 mg levodopa per mL. Tablets:
monary, renal/hepatic impairment; active (Immediate-Release [Sinemet]): 10 mg
peptic ulcer, treated open-angle glaucoma, carbidopa/100 mg levodopa, 25 mg car-
seizure disorder, pts at risk for hypotension, bidopa/100 mg levodopa, 25 mg carbi-
elderly. dopa/250 mg levodopa. Tablets: (Orally
Disintegrating Immediate-Release): 10
ACTION
mg carbidopa/100 mg levodopa, 25 mg
Levodopa is converted to DOPamine in carbidopa/100 mg levodopa, 25 mg car-
basal ganglia, increasing DOPamine con- bidopa/250 mg levodopa.
centration in brain, inhibiting hyperactive

underlined – top prescribed drug


carbidopa/levodopa 189

Capsules: (Extended-Release [Ry- disconnecting pump. Refer to manu-


tary]): carbidopa/levodopa: 23.75 mg/95 facturer’s guidelines for morning dose,
mg, 36.25 mg/145 mg, 48.75 mg/195 mg, continuous dose escalation, titration
61.25 mg/245 mg. Tablets: (Extended-Re- instructions. C
lease [Sinemet CR]): 25 mg carbidopa/100
mg levodopa, 50 mg carbidopa/200 mg Dosage in Renal/Hepatic Impairment
levodopa. Use caution.

ADMINISTRATION/HANDLING SIDE EFFECTS


Note: Space doses evenly over waking Frequent (80%–50%): Involuntary move-
hours. ments of face, tongue, arms, upper
body; nausea/vomiting; anorexia. Occa-
Enteral Suspension sional: Depression, anxiety, confusion,
Refrigerate. Remove 20 min prior to ad- nervousness, urinary retention, pal-
ministration. pitations, dizziness, light-headedness,
decreased appetite, blurred vision,
PO constipation, dry mouth, flushed skin,
• Scored tablets may be crushed. • Give headache, insomnia, diarrhea, unusual
with meals to decrease GI upset. • Do fatigue, darkening of urine and sweat.
not crush or chew extended-release tab- Rare: Hypertension, ulcer, hemolytic
lets. anemia (marked by fatigue).
PO ADVERSE EFFECTS/TOXIC
• (Parcopa): Place orally disintegrating REACTIONS
tablet on top of tongue. Tablet will dissolve
in seconds; pt to swallow with saliva. Not High incidence of involuntary choreiform,
necessary to administer with liquid. dystonic, dyskinetic movements in those
on long-term therapy. Numerous mild to
INDICATIONS/ROUTES/DOSAGE severe CNS and psychiatric disturbances
Parkinsonism may occur (reduced attention span,
anxiety, nightmares, daytime drowsiness,
PO: ADULTS, ELDERLY (IMMEDIATE-­
euphoria, fatigue, paranoia, psychotic epi-
RELEASE ORALLY DISINTEGRATING TABLET):
sodes, depression, hallucinations).
Initially, 25/100 mg 3 times/day. May in-
crease daily or every other day by 1 tablet NURSING CONSIDERATIONS
up to 200/2,000 mg daily. (EXTENDED-
RELEASE): (Sinemet CR) 50/200 mg 2 BASELINE ASSESSMENT
times/day at least 6 hrs apart. Intervals Assess symptoms of Parkinson’s disease
between doses of Sinemet CR should be (e.g., rigidity, pill rolling, gait). Receive
4–8 hrs while awake, with smaller doses full medication history and screen for
at end of day if doses are not equal. May interactions.
adjust q3days. Maximum: 8 tablets/
day. (Rytary): Initially, 23.75/95 mg 3 INTERVENTION/EVALUATION
times/day for 3 days, then to 36.25/145 Be alert to neurologic effects (headache,
mg 3 times/day. Frequency may be in- lethargy, mental confusion, agitation).
creased to maximum of 5 times/day if Monitor for evidence of dyskinesia (diffi-
needed and tolerated. Maximum daily culty with movement). Assess for clinical
dose: 612.5/2450 mg/day. (Enteral reversal of symptoms (improvement of
Suspension): Maximum: 2000 mg (1 tremor of head and hands at rest, mask-
container) over 16 hrs through NJ or like facial expression, shuffling gait, mus-
PEG tube via infusion pump. Also take cular rigidity). Monitor B/P (standing,
oral immediate-release in evening after sitting, supine).

Canadian trade name Non-Crushable Drug High Alert drug


190 CARBOplatin
PATIENT/FAMILY TEACHING PRECAUTIONS
• Avoid tasks that require alertness, mo- Contraindications: Hypersensitivity to
tor skills until response to drug is estab- CARBOplatin. History of severe allergic
C lished. • Sugarless gum, sips of water reaction to CISplatin, platinum com-
may relieve dry mouth. • Take with pounds, mannitol; severe bleeding, se-
food to minimize GI upset. • Effects vere myelosuppression. Cautions: Mod-
may be delayed from several wks to erate bone marrow depression, renal
mos. • May cause darkening of urine impairment, elderly.
or sweat (not harmful). • Report any
uncontrolled movement of face, eyelids, ACTION
mouth, tongue, arms, hands, legs; mental Inhibits DNA synthesis by cross-linking
changes; palpitations; severe or persis- with DNA strands, preventing cell divi-
tent nausea/vomiting; difficulty urinat- sion. Therapeutic Effect: Interferes
ing. • Report exacerbations of asthma, with DNA function.
underlying depression, psychosis.
PHARMACOKINETICS
Protein binding: Low. Hydrolyzed in solu-
CARBOplatin tion to active form. Primarily excreted in
urine. Half-life: 2.6–5.9 hrs.
kar-boe-plat-in LIFESPAN CONSIDERATIONS
(CARBOplatin Injection )
Pregnancy/Lactation: If possible,
j BLACK BOX ALERT jMust be avoid use during pregnancy, esp. first tri-
administered by personnel trained
in administration/handling of chem- mester. May cause fetal harm. Unknown if
otherapeutic agents (high potential distributed in breast milk. Breastfeeding
for severe reactions, including not recommended. Children: Safety and
anaphylaxis [may occur within min- efficacy not established. Elderly: Pe-
utes of administration] and sudden ripheral neurotoxicity increased, myelo-
death). Profound myelosuppression
(anemia, thrombocytopenia) has toxicity may be more severe. Age-related
occurred. Vomiting may occur. renal impairment may require decreased
Do not confuse CARBOplatin with dosage, careful monitoring of blood
CISplatin or oxaliplatin, or with counts.
Platinol.
INTERACTIONS
uCLASSIFICATION DRUG: Bone marrow depressants
PHARMACOTHERAPEUTIC: Alkylat- (e.g., cladribine) may increase myelo-
ing agent. Platinum analog. CLINI- suppression. May increase adverse effects
CAL: Antineoplastic. of cloZAPine, natalizumab, lefluno-
mide. May increase immunosuppressive
effect of baricitinib, fingolimod. May
USES increase concentration/effect of bexaro-
Treatment of advanced ovarian carci- tene. May decrease therapeutic effect of
noma. Palliative treatment of recur- BCG (intravesical), vaccines (live).
rent ovarian cancer. OFF-LABEL: Brain May increase adverse effects of vac-
tumors, Hodgkin’s and non-Hodgkin’s cines (live). HERBAL: None significant.
lymphomas, malignant melanoma, reti- Echinacea may decrease level/effects.
noblastoma; treatment of breast, bladder, FOOD: None known. LAB VALUES: May
cervical, endometrial, esophageal, small- decrease serum calcium, magnesium,
cell lung, non–small-cell lung, head and potassium, sodium. May increase serum
neck, testicular carcinomas; germ cell BUN, alkaline phosphatase, bilirubin,
tumors, osteogenic sarcoma. creatinine, AST.
underlined – top prescribed drug
CARBOplatin 191

AVAILABILITY (Rx) Creatinine Clearance Dosage Day 1


10 mg/mL (5 mL, 15
Injection Solution: 60 mL/min or greater 360 mg/m2
mL, 45 mL, 60 mL). 41–59 mL/min 250 mg/m2
16–40 mL/min 200 mg/m2 C
ADMINISTRATION/HANDLING
b ALERT c May be carcinogenic, muta- Dosage in Hepatic Impairment
genic, teratogenic. Handle with extreme No dose adjustment.
care during preparation/administration.
SIDE EFFECTS
IV
Frequent (80%–65%): Nausea, vomiting.
Reconstitution • Dilute with D5W or Occasional (17%–4%): Generalized pain,
0.9% NaCl to a final concentration as low diarrhea/constipation, peripheral neu-
as 0.5 mg/mL. ropathy. Rare (3%–2%): Alopecia, asthe-
Rate of administration • Infuse over nia, hypersensitivity reaction (erythema,
15–60 min. • Rarely, anaphylactic reac- pruritus, rash, urticaria).
tion occurs minutes after administration.
Use of epinephrine, corticosteroids allevi- ADVERSE EFFECTS/TOXIC
ates symptoms. REACTIONS
Storage • Store vials at room temper- Myelosuppression may be severe, re-
ature. • After dilution, solution is stable sulting in anemia, infection (sepsis,
for 8 hrs. pneumonia), major bleeding. Prolonged
treatment may result in peripheral neu-
IV INCOMPATIBILITIES rotoxicity.
Amphotericin B complex (Abelcet, AmBi-
some, Amphotec). NURSING CONSIDERATIONS
IV COMPATIBILITIES BASELINE ASSESSMENT
Etoposide (VePesid), granisetron (Ky- Obtain ECG, CBC, serum chemistries,
tril), ondansetron (Zofran), PACLitaxel renal function test. Offer emotional sup-
(Taxol), palonosetron (Aloxi). port. Do not repeat treatment until WBC
recovers from previous therapy. Trans-
INDICATIONS/ROUTES/DOSAGE fusions may be needed in pts receiving
Note: Doses commonly calculated by prolonged therapy (myelosuppression
target AUC. increased in those with previous therapy,
renal impairment).
Ovarian Carcinoma
IV: ADULTS: Target AUC 5–6 over 1 hr INTERVENTION/EVALUATION
on day 1; repeat q3 wks for 3–6 cycles Monitor pulmonary function studies,
(in combination with paclitaxel). Do not hepatic/renal function tests, CBC, serum
repeat dose until neutrophil and platelet electrolytes. Monitor for fever, sore throat,
counts are within acceptable levels. signs of local infection, unusual bruising/
Dose Modification bleeding from any site, symptoms of ane-
Platelets less than 50,000 cells/ mia (excessive fatigue, weakness).
mm3 or ANC less than 500 cells/
PATIENT/FAMILY TEACHING
mm3: Give 75% of dose.
• Nausea, vomiting generally abate
Dosage in Renal Impairment within 24 hrs. • Do not have immuniza-
Initial dosage is based on creatinine tions without physician’s approval (drug
clearance; subsequent dosages are based lowers body’s resistance). • Avoid con-
on pt’s tolerance, degree of myelosup- tact with those who have recently re-
pression. ceived live virus vaccine.
Canadian trade name Non-Crushable Drug High Alert drug
192 carfilzomib

LIFESPAN CONSIDERATIONS
carfilzomib Pregnancy/Lactation: Avoid pregnancy.
kar-fil-zoh-mib May cause fetal harm. Unknown if excreted
C
(Kyprolis) in breast milk. Children: Safety and ef-
Do not confuse carfilzomib with ficacy not established. Elderly: No age-
crizotinib, ixazomib, PAZOpanib. related precautions noted.

uCLASSIFICATION INTERACTIONS
PHARMACOTHERAPEUTIC: Protea- DRUG: May decrease levels/effects of
some inhibitor. CLINICAL: Antineo- BCG (intravesical). May increase
plastic. myelosuppressive effect of myelosup-
pressants (e.g., cladribine). Oral
contraceptives may increase risk of
USES thrombosis. HERBAL: None significant.
Treatment of pts with multiple myeloma FOOD: None known. LAB VALUES: May
who have received at least 2 prior increase serum creatinine, glucose,
therapies including bortezomib and creatinine, ALT, AST, bilirubin, calcium.
an immunomodulatory agent and have May decrease RBC, Hgb, Hct, absolute
demonstrated disease progression on neutrophil count (ANC), platelet count;
or within 60 days of completion of last serum magnesium, phosphate, potas-
therapy. In combination with dexameth- sium, sodium.
asone or lenalidomide and dexametha-
AVAILABILITY (Rx)
sone for treatment of relapsed multiple
myeloma who have received 1 to 3 prior Injection Powder for Reconstitution (Sin-
therapies. gle-Use Vial): 10 mg, 30 mg, 60 mg.

PRECAUTIONS ADMINISTRATION/HANDLING
Contraindications: Hypersensitivity to IV
carfilzomib. Cautions: Preexisting HF, Reconstitution • Reconstitute 60-mg
decreased left ventricular ejection frac- vial with 29 mL Sterile Water for Injection
tion, myocardial abnormalities, com- (30-mg vial with 15 mL, 10 mg with 5
plications of pulmonary hypertension mL), directing solution to inside wall of
(e.g., dyspnea), hepatic impairment, vial (minimizes foaming). • Swirl and
thrombocytopenia. invert vial slowly for 1 min or until com-
ACTION pletely dissolved. • Do not shake. • If
foaming occurs, rest vial for 2–5 min
Blocks action of proteasomes (respon- until subsided. • Withdraw calculated
sible for intracellular protein homeosta- dose from vial and dilute into 50–100 mL
sis). Therapeutic Effect: Produces cell D5W (depending on dose and infusion
cycle arrest and apoptosis. duration). • Final concentration of re-
PHARMACOKINETICS constituted solution: 2 mg/mL.
Rate of administration • Infuse over
Protein binding: 97%. Rapidly, exten- 10–30 min (depending on the dose regi-
sively metabolized. Excreted primarily men) via dedicated IV line. Flush line
extrahepatically. Minimal removal by before and after with NaCl or D5W. • Do
hemodialysis. Half-life: Equal to or less not administer as a bolus.
than 1 hr on day 1 of cycle 1. Proteasome Storage • Refrigerate undiluted vials.
inhibition was maintained for 48 hrs or • Reconstituted solution may be refriger-
longer following first dose of carfilzomib ated up to 24 hrs. • At room tempera-
for each week of dosing. ture, use diluted solution within 4 hrs.
underlined – top prescribed drug
carfilzomib 193

IV INCOMPATIBILITIES over 30 min on days 1, 2, 15, and 16 of a


Do not mix with other IV medications or 28-day cycle. Continue until disease pro-
additives. Flush IV administration line gression or unacceptable toxicity.
with NaCl or D5W immediately before and C
Multiple Myeloma, Relapsed/Refractory
after carfilzomib administration.
(In Combination with Lenalidomide and
INDICATIONS/ROUTES/DOSAGE Dexamethasone)
IV infusion: ADULTS, ELDERLY: Cycle 1: 20
b ALERT c Dose is calculated using pt’s
mg/m2 over 10 min on days 1 and 2. If tol-
actual body surface area at baseline. Pts
erated, increase to 27 mg/m2 over 10 min
with a body surface area greater than 2.2
on days 8, 9, 15, and 16 of a 28-day cycle.
m2 should receive dose based on a body
Cycles 2–12: 27 mg/m2 over 10 min on
surface area of 2.2 m2. No dose adjust-
days 1, 2, 8, 9, 15, and 16 of a 28-day cy-
ment needed for weight changes of less
cle. Cycles 13–18: 27 mg/m2 over 10 min
than or equal to 20%.
on days 1, 2, 15, and 16 of a 28-day cycle.
b ALERT c Prior to each dose in cycle 1,
Beginning with cycle 19, lenalidomide
give 250 mL to 500 mL NaCl bolus. Give an
and dexamethasone may be continued
additional 250 mL to 500 mL IV fluid fol-
(until disease progression or unaccept-
lowing administration. Continue IV hydra-
able toxicity) without carfilzomib.
tion in subsequent cycles (reduces risk of
renal toxicity, tumor lysis syndrome). Pre- Multiple Myeloma, Relapsed/Refractory
medicate with dexamethasone 4 mg PO (in Combination with Dexamethasone)
or IV prior to all doses during cycle 1 IV infusion: ADULTS, ELDERLY: Cycle 1:
and prior to all doses during first cycle of 20 mg/m2 over 30 min on days 1 and 2.
dose escalation to 27 mg/m2 (reduces If tolerated, increase to 56 mg/m2 over 30
incidence, severity of infusion reactions). min on days 8, 9, 15, and 16 of a 28-day
Reinstate dexamethasone premedication cycle. Cycle 2 and beyond: 56 mg/m2 over
(4 mg PO or IV) if symptoms develop or 30 min on days 1, 2, 8, 9, 15, and 16 of
reappear during subsequent cycles. a 28-day cycle. Continue until disease pro-
gression or unacceptable toxicity.
Multiple Myeloma, Relapsed/Refractory
(Single-Agent 20/27 mg/m2 Regimen) Multiple Myeloma, Relapsed/Refractory
IV infusion: ADULTS, ELDERLY: Cycle 1: 20 (in Combination with Dexamethasone;
mg/m2 over 10 min on days 1 and 2. If 20/70 mg/m2 Regimen [once-wkly dosing])
tolerated, increase to 27 mg/m2 over 10 IV infusion: ADULTS, ELDERLY: Cycle 1: 20
min on days 8, 9, 15, and 16 of a 28-day mg/m2 over 30 min on day 1. Increase
cycle. Cycles 2–12: 27 mg/m2 over 10 dose to 70 mg/m2 over 30 min on days 8
min on days 1, 2, 8, 9, 15, and 16 of a and 15 of a 28-day treatment cycle. Cycle
28-day cycle. Cycles 13 and beyond: 27 2 and beyond: 70 mg/m2 over 30 min on
mg/m2 over 10 min on days 1, 2, 15, and days 1, 8, and 15 of a 28-day treatment
16 of a 28-day cycle. Continue until dis- cycle. Continue until disease progression
ease progression or unacceptable toxicity. or unacceptable toxicity.
Multiple Myeloma, Relapsed/Refractory Dose Modification
(Single-Agent 20/56 mg/m2 Regimen) Hematologic
IV infusion: ADULTS, ELDERLY: Cycle 1: 20 Grade 3 or 4 neutropenia: Withhold
mg/m2 over 30 min on days 1 and 2. If tol- dose. Continue at same dose if fully re-
erated, increase to 56 mg/m2 over 30 min covered prior to next scheduled dose. If
on days 8, 9, 15, and 16 of a 28-day cycle. recovered to Grade 2, reduce dose by one
Cycles 2–12: 56 mg/m2 over 30 min on dose level. If dose tolerated, may escalate
days 1, 2, 8, 9, 15, and 16 of a 28-day to previous dose. Grade 4 thrombo-
cycle. Cycles 13 and beyond: 56 mg/m2 cytopenia: Withhold dose. Continue at

Canadian trade name Non-Crushable Drug High Alert drug


194 carfilzomib
same dose if fully recovered prior to next headache, cough, peripheral edema, vom-
scheduled dose. If recovered to Grade 3, iting, constipation, back pain. Occasional
reduce dose by one dose level. If dose (18%–14%): Insomnia, chills, arthralgia,
C tolerated, may escalate to previous dose. muscle spasms, hypertension, asthenia,
extremity pain, dizziness, hypoesthesia
Cardiac (decreased sensitivity to touch), anorexia.
Grade 3 or 4, new onset or wors-
ening of HF, decreased LVF, myo- ADVERSE EFFECTS/TOXIC
cardial ischemia: Withhold dose until REACTIONS
resolved or at baseline. After resolution, Pneumonia (10% of pts), acute renal fail-
restart at reduced dose level. If dose tol- ure (4% of pts), pyrexia (3% of pts), and
erated, may escalate to previous dose. HF (3% of pts) were reported. Adverse
reactions leading to discontinuation oc-
Hepatic
curred in 15% of pts. Upper respiratory
Grade 3 or 4 elevation of bilirubin,
tract infection reported in 28% of pts. HF,
transaminases: Withhold dose until
pulmonary edema, decrease in ejection
resolved or at baseline. After resolution, fraction were reported in 7% of pts. Infu-
restart at reduced dose level. If dose tol- sion reaction characterized by chills, fever,
erated, may escalate to previous dose. wheezing, facial flushing, dyspnea, vomit-
Peripheral Neuropathy ing, chest tightness can occur immediately
Grade 3 or 4: Withhold dose until re- following or up to 24 hrs after administra-
solved or at baseline. After resolution, tion. Tumor lysis syndrome occurs rarely.
restart at reduced dose level. If dose NURSING CONSIDERATIONS
tolerated, may escalate to previous dose.
BASELINE ASSESSMENT
Pulmonary Toxicity
Obtain accurate height and weight. Ob-
Pulmonary hypertension: Withhold tain full history of home medications
dose until resolved or at baseline. After including vitamins, herbal products.
resolution, restart at reduced dose level. Ensure hydration status and maintain
If dose tolerated, may escalate to previ- throughout treatment. Obtain CBC, se-
ous dose. Grade 3 or 4 pulmonary rum chemistries. Assess vital signs, O2
complications: Withhold dose until
saturation. Platelet nadirs occur around
resolved or at baseline. After resolution, day 8 of each 28-day cycle and recover to
restart at reduced dose level. If dose tol- baseline by start of the next 28-day cycle.
erated, may escalate to previous dose.
INTERVENTION/EVALUATION
Renal Toxicity
Monitor for fluid overload. Monitor plate-
Serum creatinine 2 times or greater
let count frequently; adjust dose accord-
from baseline: Withhold dose until
ing to grade of thrombocytopenia. Obtain
renal function improves to Grade 1 or serum ALT, AST, bilirubin for evidence of
baseline. Withhold dose until resolved hepatotoxicity. Monitor vital signs, O2 satu-
or at baseline. After resolution, restart at ration routinely. Monitor cardiac function
reduced dose level. If dose tolerated, may and manage as needed. Assess for palpi-
escalate to previous dose. tations, tachycardia. Assess for anemia-
Dosage in Renal/Hepatic Impairment related dizziness, exertional dyspnea,
No dose adjustment. fatigue, weakness, syncope. Report de-
creases in Hgb, Hct, platelets, neutrophils.
SIDE EFFECTS Monitor for acute infection (fever, diapho-
Frequent (56%–20%): Fatigue, anemia, resis, lethargy, oral mucosal changes, pro-
nausea, exertional dyspnea, diarrhea, fever, ductive cough), bloody stools, bruising,

underlined – top prescribed drug


cariprazine 195
hematuria, DVT, pulmonary embolism. neutropenia; hx of drug-induced leuko-
Encourage nutritional intake and assess penia, neutropenia; debilitated, diabetes
anorexia, weight loss. Reinforce birth con- mellitus, dyslipidemia, elderly, hepatic
trol compliance. Monitor daily pattern of impairment, Parkinson’s disease, pts at C
bowel activity, stool consistency. Offer anti- risk for hypotension (dehydration, hypo-
emetics if nausea, vomiting occur. Monitor volemia, concomitant use of antihyper-
for symptoms of neutropenia. tensives), pts at risk for aspiration, dys-
phagia; history of cardiovascular disease
PATIENT/FAMILY TEACHING
(e.g., ischemic heart disease, HF, cardiac
• Blood tests will be drawn rou- arrhythmias); pts at risk for CVA, TIA; hx
tinely. • Immediately report any newly of seizures. Concomitant use of medica-
prescribed medications. • May alter taste tions that lower seizure threshold. Avoid
of food or decrease appetite. • Report concomitant use of CYP3A inducers.
bloody stool/urine, increased bruising,
difficulty breathing, weakness, dizziness, ACTION
palpitations, weight loss. • Maintain strict Exact mechanism unknown. Partial ago-
oral hygiene. • Do not have immuniza- nist of central DOPamine D2 and sero-
tions without physician approval (drug tonin 5-HT1A receptors and antagonist
lowers body’s resistance). • Avoid those of serotonin 5-HT2A receptors. Thera-
who have recently taken live virus vac- peutic Effect: Diminishes symptoms of
cine. • Avoid crowds, those with symp- psychotic behavior.
toms of viral illness.
PHARMACOKINETICS
Widely distributed. Metabolized in liver.
cariprazine Protein binding: 91%–97%. Peak plasma
concentration: 3–6 hrs. Mean plasma
kar-ip-ra-zeen concentrations decrease approx. 50% af-
(Vraylar) ter 1 wk from last dose. Excreted primar-
j BLACK BOX ALERT j Elderly ily in urine (21%). Half-life: 2–4 days.
pts treated with antipsychotic drugs
are at an increased risk of death. LIFESPAN CONSIDERATIONS
Treatment not approved in pts with
dementia-related psychosis. Pregnancy/Lactation: Avoid preg-
Do not confuse cariprazine with nancy; may cause fetal harm. May increase
Compazine or mirtazapine. risk of extrapyramidal symptoms and/or
withdrawal syndrome in neonates. Un-
uCLASSIFICATION known if distributed in breast milk. Must
PHARMACOTHERAPEUTIC: Sero- either discontinue drug or discontinue
tonin receptor antagonist. CLINI- breastfeeding. Children: Safety and ef-
CAL: Second-generation (atypical) ficacy not established. Elderly: May in-
antipsychotic. crease risk of adverse effects due to age-
related cardiac/hepatic/renal impairment.
USES INTERACTIONS
Treatment of schizophrenia. Acute treat- DRUG: Strong CYP3A inhibitors
ment of manic or mixed episodes and (e.g., clarithromycin, ketoconazole,
major depression associated with bipolar ritonavir) may increase concentration/
I disorder. effect. Strong CYP3A inducers (e.g.,
carBAMazepine, rifampin), moder-
PRECAUTIONS ate CYP3A inducers (e.g., nafcillin)
Contraindications: Hypersensitivity to car- may decrease concentration/effect; avoid
iprazine. Cautions: Baseline leukopenia, use. Alcohol, antidepressants (e.g.,

Canadian trade name Non-Crushable Drug High Alert drug


196 cariprazine
sertraline, nortriptyline), benzodi- adjust dosing to every other day. If the
azepines (e.g., diazePAM, LORaz- strong CYP3A inhibitor is discontinued,
epam), opioids (e.g., morphine), cariprazine may need to be increased. Pts
C phenothiazines (e.g., thioridazine), starting cariprazine while on CYP3A
sedative/hypnotics (e.g., zolpidem) inhibitor: 1.5 mg once on day 1; no dose
may increase CNS depression. Metoclo- on day 2; 1.5 mg once on day 3. After day 3,
pramide may increase adverse effects. increase dose to 3 mg once daily as toler-
HERBAL: St. John’s wort may decrease ated. If strong CYP3A inhibitor is discontin-
concentration/effect. Herbs with seda- ued, cariprazine may need to be increased.
tive properties (e.g., chamomile,
kava kava, valerian) may increase CNS Bipolar I (Major Depression)
depression. FOOD: Grapefruit products PO: ADULTS, ELDERLY: Initially: 0.5–1.5
may increase concentration/effect. LAB mg once daily; increase based on re-
VALUES: May increase serum ALT, AST; sponse and tolerability to 3 mg on day 15.
CPK. May decrease serum sodium. Maximum: 3 mg/day.

AVAILABILITY (Rx) Dosage in Renal Impairment


Mild to moderate impairment: No
Capsules: 1.5 mg, 3 mg, 4.5 mg, 6 mg. dose adjustment. Severe impairment:
ADMINISTRATION/HANDLING Treatment not recommended.
PO Dosage in Hepatic Impairment
Give without regard to food. Administer Mild to moderate impairment: No
whole; do not break, crush, cut, or open dose adjustment. Severe impairment:
capsule. Treatment not recommended.
INDICATIONS/ROUTES/DOSAGE
Schizophrenia SIDE EFFECTS
PO: ADULTS, ELDERLY: Initially, 1.5 mg Frequent (26%–11%): Bradykinesia, cog­
once daily. May increase to 3 mg on day wheel rigidity, drooling, dyskinesia,
2 if tolerated. May further increase in masked faces, muscle rigidity, dystonia,
increments of 1.5–3 mg based on clini- tremor, salivary hypersecretion, torticol-
cal response and tolerability. Note: Due lis, trismus, insomnia, akathisia, head-
to long half-life, changes in dosage will ache. Occasional (5%–3%): Nausea, con-
not be reflected in plasma for several stipation, restlessness, vomiting, dizziness,
wks. Range: 1.5–6 mg once daily. agitation, anxiety, dyspepsia, abdominal
pain, diarrhea, fatigue, asthenia, back
Bipolar I Disorder (Manic or Mixed pain, toothache, hypertension, decreased
Episodes) appetite. Rare (2%–1%): Dry mouth,
PO: ADULTS, ELDERLY: 1.5 mg once on day weight gain, extremity pain, somnolence,
1, then increase to 3 mg once daily on day sedation, cough, tachycardia, arthralgia.
2. May further increase in increments of
1.5–3 mg based on clinical response and ADVERSE EFFECTS/TOXIC
tolerability. Range: 3–6 mg once daily. REACTIONS
Concomitant Use of Strong CYP3A May increase risk of hypotension, ortho-
Inhibitors static hypotension, syncope; diabetes mel-
Pts starting strong CYP3A inhibi- litus, DKA, hyperglycemia, hyperglycemic
tor while on stable dose of caripra- hyperosmolar nonketotic coma; leuko-
zine: Reduce maintenance cariprazine penia, neutropenia, febrile neutropenia;
dose by 50%. Pts taking cariprazine 4.5 aspiration, dysphagia, gastritis, gastric re-
mg/day should reduce dosage to 1.5 mg/ flux; extrapyramidal symptoms including
day or 3 mg/day. Pts taking 1.5 mg/day, akathisia, dystonia, parkinsonism, tardive
underlined – top prescribed drug
carmustine 197
dyskinesia; suicidal ideation. May cause i­ncrease blood sugar levels. Monitor for
neuroleptic malignant syndrome (NMS), blurry vision, confusion, frequent urina-
manifested by altered mental status, car- tion, fruity-smelling breath, thirst, weak-
diac arrhythmias, diaphoresis, labile ness. • Treatment may cause fetal harm. C
blood pressure, malignant hyperthermia, Avoid pregnancy. Do not breast-
muscle rigidity, rhabdomyolysis, renal fail- feed. • Treatment may lower ability to
ure. May increase risk of death in pts with fight infection. • Swallow capsules whole;
dementia-related psychosis. Cognitive and do not chew, crush, cut, or open cap-
motor impairment reported in 7% of pts. sules. • Do not ingest grapefruit products
May increase seizure-like activity related to or herbal products. Report drooling, mus-
decrease in seizure threshold. Infectious cle rigidity, lockjaw, tremors, or inability to
processes including nasopharyngitis, uri- control muscle movements. • Treatment
nary tract infection reported in 1% of pts. may increase risk of seizures. • Report
Hypersensitivity reactions including angio- confusion, palpitations, profuse sweating,
edema, rash, pruritus have occurred. fluctuating blood pressure, unusually high
core body temperature, muscle rigidity,
NURSING CONSIDERATIONS dark-colored urine or decreased urine
BASELINE ASSESSMENT output; may indicate life-threatening neu-
rologic event called neuroleptic malignant
Obtain baseline fasting lipid profile, fasting syndrome (NMS).
plasma glucose level, vital signs; Hgb A1c in
pts with diabetes; ANC, CBC in pts with base-
line leukopenia, neutropenia. Receive full
medication history, including herbal prod-
carmustine
ucts, and screen for interactions. Assess ap- kar-mus-teen
pearance, behavior, speech pattern, levels (BiCNU, Gliadel Wafer)
of interest. Verify pregnancy status. Ques-
tion history of diabetes, cardiovascular dis-
j BLACK BOX ALERT j Profound
myelosuppression (leukopenia,
ease, CVA, dysphagia, hepatic impairment, thrombocytopenia) is major toxicity.
hypersensitivity reaction, TIA, seizures. High risk of pulmonary toxicity.
Must be administered by personnel
INTERVENTION/EVALUATION trained in administration/handling
Monitor ANC, CBC, fasting lipid profile, of chemotherapeutic agents (high
potential for severe reactions, in-
fasting plasma glucose levels periodically. cluding anaphylaxis, sudden death).
Assess mental status for anxiety, depres- Do not confuse carmustine with
sion, suicidal ideation (esp. at initiation bendamustine or lomustine.
and with change in dosage), social func-
tion. Due to long half-life, any change uCLASSIFICATION
in dosage will not be fully reflected for PHARMACOTHERAPEUTIC: Alkylat-
several wks; monitor closely for adverse ing agent, nitrosourea. CLINICAL:
effects during the following wks. Monitor Antineoplastic.
for hypersensitivity reaction, dysphagia,
tardive dyskinesia, extrapyramidal symp-
toms, metabolic changes including hy- USES
perglycemia. Screen for infection. Moni- BiCNU: Treatment of brain tumors,
tor for neuroleptic malignant syndrome. Hodgkin’s lymphomas (relapsed/refrac-
PATIENT/FAMILY TEACHING tory), non-Hodgkin’s lymphomas (re-
lapsed/refractory), multiple myeloma.
• Immediately report thoughts of suicide
Gliadel Wafer: Adjunct to surgery and
or plans to commit suicide. • Avoid tasks
radiation in treatment of newly diagnosed
that require alertness until response to
high-grade malignant glioma. Adjunct to
drug is established. • Therapy may
Canadian trade name Non-Crushable Drug High Alert drug
198 carmustine
surgery to prolong survival in recurrent IV
glioblastoma multiforme. OFF-LABEL:
Treatment of mycosis fungoides (topical). Reconstitution • Reconstitute 100-
C mg vial with 3 mL sterile dehydrated
PRECAUTIONS (absolute) alcohol, followed by 27 mL
Contraindications: Hypersensitivity to car- Sterile Water for Injection to provide
mustine. Cautions: Thrombocytopenia, leu- concentration of 3.3 mg/mL. • Further
kopenia, anemia, renal/hepatic impairment. dilute with 50–250 mL D5W to final con-
centration of 0.2–1 mg/mL.
ACTION Rate of administration • Infuse
Inhibits DNA, RNA synthesis by cross- over 1–2 hrs (shorter duration may
linking with DNA, RNA strands, pre- produce intense burning pain at injec-
venting cell division. Cell cycle–phase tion site, intense flushing of skin, con-
nonspecific. Therapeutic Effect: Inter- junctiva). • Flush IV line with 5–10
feres with DNA, RNA function. mL 0.9% NaCl or D5W before and after
administration to prevent irritation at
PHARMACOKINETICS injection site.
Crosses blood-brain barrier. Metabo- Storage • Refrigerate unused vi-
lized in liver. Excreted in urine. Half- als. • Reconstituted vials are stable for 8
life: 15–30 min. hrs at room temperature or 24 hrs if refrig-
erated. • Solutions further diluted with
LIFESPAN CONSIDERATIONS D5W are stable for 8 hrs at room tempera-
Pregnancy/Lactation: Avoid preg- ture. • Solutions appear clear, colorless
nancy, particularly first trimester; may to yellow. • Discard if precipitate forms,
cause fetal harm. Unknown if distributed color change occurs, or oily film develops
in breast milk. Breastfeeding not recom- on bottom of vial. • (Gliadel Wafers):
mended. Children: Safety and efficacy Store at or below −20°C (−4°F). Un-
not established. Elderly: No age-related opened pouches may be kept at room
precautions noted. temperature for maximum of 6 hrs.
INTERACTIONS IV INCOMPATIBILITIES
DRUG: Bone marrow depressants Allopurinol (Aloprim), sodium bicar-
(e.g., cladribine) may enhance myelo- bonate.
suppressive effect. Live virus vaccines
may potentiate virus replication, increase IV COMPATIBILITIES
vaccine side effects, decrease pt’s antibody Granisetron (Kytril), ondansetron (Zofran).
response to vaccine. HERBAL: Echinacea
may decrease effects. FOOD: None known. INDICATIONS/ROUTES/DOSAGE
LAB VALUES: May increase serum BUN, b ALERT c Refer to individual oncology
alkaline phosphatase, bilirubin, ALT, AST. protocols.
AVAILABILITY (Rx) Brain Tumors, Hodgkin’s Lymphoma, Non-
Injection, Powder for Reconstitution: Hodgkin’s Lymphoma, Multiple Myeloma
(BiCNU): 100 mg. Implant Device: (Gli- IV: (BiCNU): ADULTS, ELDERLY: 150–200
adel Wafer): 7.7 mg. mg/m2 as a single dose q6wks or 75–100
mg/m2 on 2 successive days q6wks.
ADMINISTRATION/HANDLING b ALERT c Next dosage is based on
b ALERT c May be carcinogenic, muta- clinical and hematologic response to
genic, teratogenic. Wear protective gloves previous dose (platelets greater than
during preparation of drug; may cause 100,000 cells/mm3 and leukocytes
transient burning, brown staining of skin. greater than 4,000 cells/mm3).

underlined – top prescribed drug


carvedilol 199
Glioblastoma Multiforme (Recurrent), INTERVENTION/EVALUATION
Glioma (Malignant, Newly Diagnosed Monitor renal/hepatic function tests. Ob-
High-Grade) tain CBC wkly during and for at least 6
Implantation: (Gliadel Wafer): ADULTS, wks after therapy ends. Monitor for hema- C
ELDERLY, CHILDREN: Up to 8 wafers (62.6 tologic toxicity (fever, sore throat, signs of
mg) may be placed in resection cavity. local infection, unusual bruising/bleeding
from any site), symptoms of anemia (ex-
Dosage Modification
cessive fatigue, weakness). Monitor for
Leukocytes 2,000–2,999 cells/mm3
pulmonary toxicity; observe for dyspnea,
or platelets 25,000–74,999 cells/
adventitious breath sounds.
mm3: Give 70% of dose. Leukocytes
less than 2,000 cells/mm3 or plate- PATIENT/FAMILY TEACHING
lets less than 25,000 cells/mm3: Give • Maintain adequate hydration (may
50% of dose. protect against renal impairment). • Do
not have immunizations without physi-
Dosage in Renal Impairment
cian’s approval (drug lowers body’s re-
Creatinine sistance). • Avoid contact with those
Clearance (mL/min) Dosage who have recently received live virus
46–60 80% of dose vaccine. • Report nausea, vomiting, fe-
31–45 75% of dose ver, sore throat, chills, unusual bleeding/
Less than 31 Not recommended
bruising.
Dosage in Hepatic Impairment
Use caution. carvedilol
SIDE EFFECTS
Frequent: Nausea, vomiting (may last up kar-ve-dil-ole
to 6 hrs). Occasional: Diarrhea, esopha- (Apo-Carvedilol , Coreg, Coreg
gitis, anorexia, dysphagia, hyperpigmen- CR, Novo-Carvedilol )
tation. Rare: Thrombophlebitis, burning Do not confuse carvedilol with
sensation, pain at injection site. atenolol or carteolol, or Coreg
with Corgard, Cortef, or Cozaar.
ADVERSE EFFECTS/TOXIC
REACTIONS uCLASSIFICATION

Hematologic toxicity due to myelosup- PHARMACOTHERAPEUTIC: Beta-


pression occurs frequently. Thrombocy- adrenergic blocker. CLINICAL: Anti-
topenia occurs approximately 4 wks after hypertensive.
treatment begins and lasts 1–2 wks. Leu-
kopenia is evident 5–6 wks after treat- USES
ment begins and lasts 1–2 wks. Anemia Treatment of mild to severe HF, left ven-
occurs less frequently. Mild, reversible tricular dysfunction following MI, hyper-
hepatotoxicity occurs frequently. Pro- tension. OFF-LABEL: Treatment of angina
longed, high-dose therapy may produce pectoris, idiopathic cardiomyopathy.
impaired renal function, pulmonary tox-
icity (pulmonary infiltrate/fibrosis). PRECAUTIONS
Contraindications: Hypersensitivity to
NURSING CONSIDERATIONS
carvedilol. Bronchial asthma or related
BASELINE ASSESSMENT bronchospastic conditions, cardiogenic
Obtain CBC, renal/hepatic function stud- shock, decompensated HF requiring intra-
ies before initiation and periodically venous inotropic therapy, severe hepatic
thereafter. Offer emotional support. impairment, second- or third-degree AV

Canadian trade name Non-Crushable Drug High Alert drug


200 carvedilol
block, severe bradycardia, or sick sinus may enhance slowing of HR or cardiac
syndrome (except in pts with pacemaker). conduction. May decrease bronchodilation
Cautions: Diabetes, myasthenia gravis, effect of beta2 agonists (e.g., albuterol,
C mild to moderate hepatic impairment. salmeterol). May increase concentration/
Withdraw gradually to avoid acute tachy- effect of pazopanib, topotecan. Riv-
cardia, hypertension, and/or ischemia. Pts astigmine may increase risk of bradycar-
suspected of having Prinzmetal’s angina, dia. HERBAL: Herbals with hypertensive
pheochromocytoma, hx of severe anaphy- properties (e.g., licorice, yohimbe)
laxis to allergens. or hypotensive properties (e.g., gar-
lic, ginger, ginkgo biloba) may alter
ACTION effects. FOOD: None known. LAB VALUES:
Possesses nonselective beta-blocking and May increase serum creatinine, bilirubin,
alpha-adrenergic blocking activity. Causes ALT, AST, PT.
vasodilation. Therapeutic Effect: Hy-
pertension: Reduces cardiac output, AVAILABILITY (Rx)
exercise-induced tachycardia, reflex Tablets (Immediate-Release): 3.125 mg,
orthostatic tachycardia; reduces periph- 6.25 mg, 12.5 mg, 25 mg.
eral vascular resistance. HF: Decreases Capsules: (Extended-Release [Coreg
pulmonary capillary wedge pressure, CR]): 10 mg, 20 mg, 40 mg, 80 mg.
heart rate, systemic vascular resistance;
increases stroke volume index. ADMINISTRATION/HANDLING
PO
PHARMACOKINETICS • Give with food (slows rate of absorption,
Route Onset Peak Duration reduces risk of orthostatic effects). • Do
PO 30 min 1–2 hrs 24 hrs not crush or cut extended-release cap-
sules. • Capsules may be opened and
Rapidly, extensively absorbed from GI sprinkled on applesauce for immediate use.
tract. Protein binding: 98%. Metabolized
in liver. Excreted primarily via bile into INDICATIONS/ROUTES/DOSAGE
feces. Minimally removed by hemodi- Hypertension
alysis. Half-life: 7–10 hrs. Food delays PO: (Immediate-Release): ADULTS,
rate of absorption. ELDERLY: Initially, 6.25 mg twice daily.
LIFESPAN CONSIDERATIONS May double at intervals of 1–2 wks to
12.5 mg twice daily, then to 25 mg twice
Pregnancy/Lactation: Unknown if daily. Maximum: 25 mg twice daily.
drug crosses placenta or is distributed in (Extended-Release): Initially, 20 mg
breast milk. May produce bradycardia, once daily. May increase to 40 mg once
apnea, hypoglycemia, hypothermia dur- daily after 1–2 wks, then to 80 mg once
ing delivery; may contribute to low birth- daily. Maximum: 80 mg once daily.
weight infants. Children: Safety and effi-
cacy not established. Elderly: Incidence HF
of dizziness may be increased. PO: (Immediate-Release): ADULTS, EL-
DERLY: Initially, 3.125 mg twice daily. May
INTERACTIONS double at 2-wk intervals to highest toler-
DRUG: Calcium channel blockers ated dosage. Maximum: WEIGHING MORE
(e.g., diltiaZEM, verapamil), digoxin, THAN 85 KG: 50 mg twice daily; LESS THAN
CYP2C9 inhibitors (e.g., amiodarone, 85 KG: 25 mg twice daily. (Extended-
fluconazole) increase risk of cardiac Release): Initially, 10 mg once daily for
conduction disturbances. CYP2D6 inhib- 2 wks. May increase to 20 mg, 40 mg, and
itors (e.g., FLUoxetine, PARoxetine) 80 mg over successive intervals of at least
may increase concentration/side effects; 2 wks. Maximum: 80 mg/day.

underlined – top prescribed drug


caspofungin 201
Left Ventricular Dysfunction Following MI B/P 1 hr after dosing as guide for toler-
PO: (Immediate-Release): ADULTS, ance. Assess pulse for quality, regularity,
ELDERLY: Initially, 3.125–6.25 mg twice rate; monitor for bradycardia. Monitor
daily. May increase at intervals of 3–10 ECG for cardiac arrhythmias. Assist with C
days up to 25 mg twice daily. Maxi- ambulation if dizziness occurs. Assess
mum: 50 mg twice daily. (Extended- for evidence of HF: dyspnea (particularly
Release): Initially, 10–20 mg once daily. on exertion or lying down), night cough,
May increase incrementally in intervals of peripheral edema, distended neck veins.
3–10 days. Target dose: 80 mg once daily. Monitor I&O (increase in weight, de-
crease in urine output may indicate HF).
Dosage in Renal Impairment Monitor renal/hepatic function tests.
No dose adjustment.
PATIENT/FAMILY TEACHING
Dosage in Hepatic Impairment • Full therapeutic effect of B/P may take
Contraindicated in severe impairment. 1–2 wks. • Contact lens wearers may
SIDE EFFECTS experience decreased lacrima-
tion. • Take with food. • Abruptly
Frequent (6%–4%): Fatigue, dizziness. stopping treatment or missing multiple
Occasional (2%): Diarrhea, bradycar- doses may cause beta-blocker with-
dia, rhinitis, back pain. Rare (less than drawal symptoms (fast heart rate, high
2%): Orthostatic hypotension, drowsi- blood pressure, palpitations, sweating,
ness, UTI, viral infection. tremors). • Compliance with therapy
ADVERSE EFFECTS/TOXIC regimen is essential to control hyperten-
REACTIONS sion. • Report excessive fatigue, pro-
longed dizziness. • Do not use nasal
Overdose may produce profound bra- decongestants, OTC cold preparations
dycardia, hypotension, bronchospasm, (stimulants) without physician’s ap-
cardiac insufficiency, cardiogenic shock, proval. • Monitor B/P, pulse before
cardiac arrest. Abrupt withdrawal may taking medication. • Restrict salt, alco-
result in diaphoresis, palpitations, head- hol intake.
ache, tremors. May precipitate HF, MI in
pts with cardiac disease; thyroid storm
in pts with thyrotoxicosis; peripheral
ischemia in pts with existing peripheral
vascular disease. Hypoglycemia may oc-
caspofungin
cur in pts with previously controlled kas-poe-fun-jin
diabetes. May mask symptoms of hypo- (Cancidas)
glycemia.
uCLASSIFICATION
NURSING CONSIDERATIONS
PHARMACOTHERAPEUTIC: Echino-
BASELINE ASSESSMENT candin antifungal. CLINICAL: Anti-
Assess B/P, apical pulse immediately be- fungal.
fore drug is administered (if pulse is 60
beats/min or less or systolic B/P is less
than 90 mm Hg, withhold medication,
USES
contact physician). Receive full medica- Treatment of invasive aspergillosis, can-
tion history and screen for interactions. didemia, Candida infection (intra-ab-
dominal abscess, peritonitis, esophageal,
INTERVENTION/EVALUATION pleural space) in pts aged 3 months and
Monitor B/P for hypotension, respira- older. Empiric therapy for presumed fun-
tions for dyspnea. Take standing systolic gal infections in febrile neutropenia.

Canadian trade name Non-Crushable Drug High Alert drug


202 caspofungin

PRECAUTIONS Rate of administration • Infuse over


Contraindications: Hypersensitivity to ca- 60 min.
spofungin. Cautions: Concurrent use of Storage • Refrigerate vials but warm
C cycloSPORINE, hepatic impairment. to room temperature before preparing
with diluent. • Reconstituted solution,
ACTION diluted solution, may be stored at room
Inhibits synthesis of glucan, a vital com- temperature for 1 hr before infu-
ponent of fungal cell wall formation, sion. • Final infusion solution can be
damaging fungal cell membrane. Thera- stored at room temperature for 24 hrs or
peutic Effect: Fungistatic. 48 hrs if refrigerated. • Discard if solu-
tion contains particulate or is discolored.
PHARMACOKINETICS
IV INCOMPATIBILITIES
Distributed in tissue. Protein binding:
97%. Metabolized in liver. Excreted in Cefepime (Maxipime), ceftaroline (Tefla-
urine (50%), feces (30%). Not removed ro), cefTAZidime (Fortaz), cefTRIAXone
by hemodialysis. Half-life: 40–50 hrs. (Rocephin), furosemide (Lasix).

LIFESPAN CONSIDERATIONS IV COMPATIBILITIES


Pregnancy/Lactation: May be embryo- Aztreonam (Azactam), DAPTOmycin
toxic. Crosses placental barrier. Distrib- (Cubicin), fluconazole (Diflucan), line-
uted in breast milk. Children: Safety and zolid (Zyvox), meropenem (Merrem IV),
efficacy not established. Elderly: Age- piperacillin/tazobactam (Zosyn), vanco-
related moderate renal impairment may mycin.
require dosage adjustment.
INDICATIONS/ROUTES/DOSAGE
INTERACTIONS Aspergillosis
DRUG: CycloSPORINE may increase Note: Continue for minimum of 6–12
concentration. RifAMPin may decrease wks.
concentration. May decrease concentra- IV: ADULTS, ELDERLY: Give single 70-mg
tion/effect of tacrolimus. May decrease loading dose on day 1, followed by 50
therapeutic effect of saccharomyces mg/day thereafter. CHILDREN 3 MOS–17
boulardii. HERBAL: None significant. YRS: 70 mg/m2 on day 1, then 50 mg/
FOOD: None known. LAB VALUES: May m2 daily. Maximum: 70 mg loading
increase serum alkaline phosphatase, dose or daily dose.
bilirubin, creatinine, ALT, AST, urine pro-
Candidemia
tein. May decrease serum albumin, bicar-
Note: Continue for at least 14 days after
bonate, potassium, magnesium; Hgb, Hct.
last positive culture.
AVAILABILITY (Rx) IV: ADULTS, ELDERLY: Initially, 70 mg on
day 1, followed by 50 mg daily. CHILDREN
Injection, Powder for Reconstitution: 50-
3 MOS–17 YRS: 70 mg/m2 on day 1, then
mg, 70-mg vials.
50 mg/m2 daily. Maximum: 70-mg
ADMINISTRATION/HANDLING loading dose, 50-mg daily dose.
IV Esophageal Candidiasis
Reconstitution • Reconstitute 50-mg Note: Continue for 7–14 days after
or 70-mg vial with 0.9% NaCl, Sterile symptom resolution.
IV: ADULTS, ELDERLY: 50 mg/day. CHIL-
Water for Injection, or Bacteriostatic Wa-
DREN 3 MOS–17 YRS: 50 mg/m2 daily.
ter for Injection. Further dilute in 0.9%
NaCl or D5W to maximum concentration Maximum: 50 mg.
of 0.5 mg/mL.

underlined – top prescribed drug


cefaclor 203
Empiric Therapy
Note: Continue for minimum 14 days if cefaclor
fungal infection confirmed (continue for
7 days after resolution of neutropenia/ sef-a-klor C
clinical symptoms). (Apo-Cefaclor , Ceclor , Novo-
IV: ADULTS, ELDERLY: Initially 70 mg, Cefaclor )
then 50 mg/day. May increase to 70 mg/ Do not confuse cefaclor with
day. CHILDREN 3 MOS–17 YRS: 70 mg/m2 cephalexin.
on day 1, then 50 mg/m2 daily. Maxi-
uCLASSIFICATION
mum: 70 mg loading dose or daily dose.
PHARMACOTHERAPEUTIC: Second-
Dosage in Renal Impairment
generation cephalosporin. CLINI-
No dose adjustment. CAL: Antibiotic.
Dosage in Hepatic Impairment
Mild: No adjustment. Moderate: CHILD-
PUGH SCORE 7–9: Decrease dose to 35 mg/ USES
day. Severe: No clinical experience. Treatment of susceptible infections due to
S. pneumoniae, S. pyogenes, S. aureus,
SIDE EFFECTS H. influenzae, E. coli, M. catarrhalis,
Frequent (26%): Fever. Occasional (11%– Klebsiella spp., P. mirabilis, including
4%): Headache, nausea, phlebitis. Rare acute otitis media, bronchitis, pharyngi-
(3% or less): Paresthesia, vomiting, di- tis/tonsillitis, respiratory tract, skin/skin
arrhea, abdominal pain, myalgia, chills, structure, UTIs.
tremor, insomnia.
PRECAUTIONS
ADVERSE EFFECTS/TOXIC
REACTIONS Contraindications: History of hypersen-
sitivity/anaphylactic reaction to cefaclor,
Hypersensitivity reaction (rash, facial cephalosporins. Cautions: Severe renal
edema, pruritus, sensation of warmth), impairment, history of penicillin allergy.
including anaphylaxis, may occur. May Extended release not approved in chil-
cause hepatic dysfunction, hepatitis dren younger than 16 yrs.
(drug-induced), or hepatic failure.
ACTION
NURSING CONSIDERATIONS Binds to bacterial cell membranes, in-
BASELINE ASSESSMENT hibits cell wall synthesis. Therapeutic
Obtain baseline CBC, BMP, LFT, serum Effect: Bactericidal.
magnesium. Determine baseline temper- PHARMACOKINETICS
ature. Question history of prior hypersen-
sitivity reaction. Well absorbed from GI tract. Protein
binding: 25%. Widely distributed. Par-
INTERVENTION/EVALUATION tially metabolized in liver. Primarily
Assess for signs/symptoms of hepatic excreted in urine. Moderately removed
dysfunction. Monitor LFT in pts with by hemodialysis. Half-life: 0.6–0.9 hr
preexisting hepatic impairment. Monitor (increased in renal impairment).
CBC, serum potassium. Monitor for fever,
LIFESPAN CONSIDERATIONS
hypersensitivity reaction.
Pregnancy/Lactation: Readily crosses
PATIENT/FAMILY TEACHING placenta. Distributed in breast milk. Chil-
• Report rash, facial swelling, itching, dif- dren: No age-related precautions noted
ficulty breathing, abdominal pain, yellowing in pts older than 1 mo. Elderly: Age-
of skin or eyes, dark-colored urine, nausea. related renal impairment may require
dosage adjustment.
Canadian trade name Non-Crushable Drug High Alert drug
204 cefadroxil

INTERACTIONS ADVERSE EFFECTS/TOXIC


DRUG: Probenecid may increase con- REACTIONS
centration. HERBAL: None significant. Antibiotic-associated colitis (abdominal
C FOOD: None known. LAB VALUES: May cramps, severe watery diarrhea, fever),
increase serum BUN, alkaline phosphatase, other superinfections may result from
bilirubin, creatinine, LDH, ALT, AST. May altered bacterial balance in GI tract.
cause positive direct/indirect Coombs’ test. Nephrotoxicity may occur, esp. in pts with
preexisting renal disease. Pts with history
AVAILABILITY (Rx) of penicillin allergy are at increased risk
Capsules: 250 mg, 500 mg. Pow- for developing a severe hypersensitivity
der for Oral Suspension:125 mg/5 mL, reaction (severe pruritus, angioedema,
250 mg/5 mL, 375 mg/5 mL. Tablets bronchospasm, anaphylaxis).
(Extended-Release): 500 mg.
NURSING CONSIDERATIONS
ADMINISTRATION/HANDLING BASELINE ASSESSMENT
PO Obtain baseline CBC, renal function tests.
• After reconstitution, oral solution is Question for history of allergies, particu-
stable for 14 days if refrigerated. • Shake larly cephalosporins, penicillins.
oral suspension well before using. • Give
without regard to food; if GI upset occurs, INTERVENTION/EVALUATION
give with food, milk. Assess oral cavity for white patches on
mucous membranes, tongue (thrush).
INDICATIONS/ROUTES/DOSAGE Monitor daily pattern of bowel activity, stool
Usual Dosage consistency. Mild GI effects may be tolerable
250–500 mg q8h
PO: ADULTS, ELDERLY: (increasing severity may indicate onset of
or 500 mg q12h (extended-release). antibiotic-associated colitis). Monitor I&O,
CHILDREN: 20–40 mg/kg/day divided renal function tests for nephrotoxicity. Be
q8–12h. Maximum: 1 g/day. alert for superinfection: fever, vomiting, di-
arrhea, anal/genital pruritus, oral mucosal
Otitis Media changes (ulceration, pain, erythema).
PO: CHILDREN:40 mg/kg/day divided
q12h. Maximum: 1 g/day. PATIENT/FAMILY TEACHING
• Continue therapy for full length of
Pharyngitis treatment. • Doses should be evenly
20 mg/kg/day divided q12h.
CHILDREN: spaced. • May cause GI upset (may
Maximum: 1 g/day. take with food, milk). • Chewable tab-
Dosage in Renal Impairment
lets must be chewed; do not swallow
Use caution. whole. • Refrigerate oral suspen-
sion. • Report persistent diarrhea.
Dosage in Hepatic Impairment
No dose adjustment. cefadroxil
SIDE EFFECTS
sef-a-drox-il
Frequent: Oral candidiasis, mild diarrhea, (Apo-Cefadroxil )
mild abdominal cramping, vaginal candidia-
sis. Occasional: Nausea, serum sickness– uCLASSIFICATION
like reaction (fever, joint pain; usually occurs PHARMACOTHERAPEUTIC: First-
after second course of therapy and resolves generation cephalosporin. CLINI-
after drug is discontinued). Rare: Allergic CAL: Antibiotic.
reaction (pruritus, rash, urticaria).

underlined – top prescribed drug


cefadroxil 205

USES ADMINISTRATION/HANDLING
Treatment of susceptible infections due PO
to group A streptococci, staphylococci, • After reconstitution, oral solution is
S. pneumoniae, H. influenzae, Klebsi- stable for 14 days if refrigerated. • Shake C
ella spp., E. coli, P. mirabilis, includ- oral suspension well before using. • Give
ing impetigo, pharyngitis/tonsillitis, without regard to food; if GI upset occurs,
skin/skin structure, UTIs. OFF-LABEL: give with food, milk.
Chronic suppression of prosthetic joint
infection. INDICATIONS/ROUTES/DOSAGE
Usual Dosage
PRECAUTIONS PO: ADULTS, ELDERLY: 1–2 g/day
Contraindications: History of hypersensi- as single dose or in 2 divided doses.
tivity/anaphylactic reaction to cefadroxil, CHILDREN: 30 mg/kg/day as a single
cephalosporins. Cautions: Severe renal dose or in 2 divided doses. Maximum:
impairment, history of penicillin allergy. 2 g/day.
History of GI disease (colitis).
Dosage in Renal Impairment
ACTION After initial 1-g dose, dosage and fre-
Binds to bacterial cell membranes, in- quency are modified based on creatinine
hibits cell wall synthesis. Therapeutic clearance and severity of infection.
Effect: Bactericidal. Creatinine Clearance Dosage
26–50 mL/min q12h
PHARMACOKINETICS 10–25 mL/min q24h
Less than 10 mL/min q36h
Well absorbed from GI tract. Protein
binding: 15%–20%. Widely distributed.
Primarily excreted in urine. Removed Dosage in Hepatic Impairment
by hemodialysis. Half-life: 1.2–1.5 hrs No dose adjustment.
(increased in renal impairment).
SIDE EFFECTS
LIFESPAN CONSIDERATIONS Frequent: Oral candidiasis, mild diar-
Pregnancy/Lactation: Readily crosses rhea, mild abdominal cramping, vagi-
placenta. Distributed in breast milk. Chil- nal candidiasis. Occasional: Nausea,
dren: No age-related precautions noted. unusual bruising/bleeding, serum sick-
Elderly: Age-related renal impairment ness–like reaction (fever, joint pain;
may require dosage adjustment. usually occurs after second course of
therapy and resolves after drug is dis-
INTERACTIONS continued). Rare: Allergic reaction
DRUG: Probenecid may increase con- (rash, pruritus, urticaria), thrombo-
centration. HERBAL: None significant. phlebitis (pain, redness, swelling at in-
FOOD: None known. LAB VALUES: May jection site).
increase serum BUN, alkaline phospha- ADVERSE EFFECTS/TOXIC
tase, bilirubin, creatinine, LDH, ALT, REACTIONS
AST. May cause positive direct/indirect
Coombs’ test. Antibiotic-associated colitis, other super-
infections (abdominal cramps, severe
AVAILABILITY (Rx) watery diarrhea, fever) may result from
altered bacterial balance in GI tract.
Capsules: 500 mg. Powder for Oral Nephrotoxicity may occur, esp. in pts with
Suspension: 250 mg/5 mL, 500 mg/5 preexisting renal disease. Pts with history
mL. Tablets: 1 g. of penicillin allergy are at increased risk

Canadian trade name Non-Crushable Drug High Alert drug


206 ceFAZolin
for developing a severe hypersensitivity and joint, genital, respiratory tract, skin/
reaction (severe pruritus, angioedema, skin structure infections; UTIs, endocar-
bronchospasm, anaphylaxis). ditis, perioperative prophylaxis, septi-
C cemia. OFF-LABEL: Prophylaxis against
NURSING CONSIDERATIONS infective endocarditis.
BASELINE ASSESSMENT
PRECAUTIONS
Obtain CBC, renal function tests. Ques- Contraindications: History of hypersensi-
tion for history of allergies, particularly tivity/anaphylactic reaction to ceFAZolin,
cephalosporins, penicillins. cephalosporins. Cautions: Severe renal
INTERVENTION/EVALUATION impairment, history of penicillin allergy,
Assess oral cavity for white patches on history of seizures.
mucous membranes, tongue (thrush). ACTION
Monitor daily pattern of bowel activity,
stool consistency. Mild GI effects may Binds to bacterial cell membranes, in-
be tolerable (increasing severity may hibits cell wall synthesis. Therapeutic
indicate onset of antibiotic-associated Effect: Bactericidal.
colitis). Monitor I&O, renal function tests PHARMACOKINETICS
for nephrotoxicity. Be alert for superin-
fection: fever, vomiting, diarrhea, anal/ Widely distributed. Protein binding: 85%.
genital pruritus, oral mucosal changes Primarily excreted unchanged in urine.
(ulceration, pain, erythema). Moderately removed by hemodialysis.
Half-life: 1.4–1.8 hrs (increased in
PATIENT/FAMILY TEACHING renal impairment).
• Continue therapy for full length of treat-
ment. • Doses should be evenly LIFESPAN CONSIDERATIONS
spaced. • May cause GI upset (may take Pregnancy/Lactation: Readily crosses
with food, milk). • Refrigerate oral sus- placenta; distributed in breast milk. Chil-
pension. • Report persistent diarrhea. dren: No age-related precautions noted.
Elderly: Age-related renal impairment
may require reduced dosage.

ceFAZolin INTERACTIONS
DRUG: Probenecid may increase con-
sef-a-zoe-lin centration. HERBAL: None significant.
Do not confuse ceFAZolin with FOOD: None known. LAB VALUES: May
cefOXitin, cefprozil, cefTRIAX- increase serum BUN, alkaline phosphatase,
one, or cephalexin. bilirubin, creatinine, LDH, ALT, AST. May
cause positive direct/indirect Coombs’ test.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: First- AVAILABILITY (Rx)
generation cephalosporin. CLINI- Injection, Powder for Reconstitution: 500
CAL: Antibiotic. mg, 1 g. Ready-to-Hang Infusion: 1 g/50
mL, 2 g/100 mL.
USES ADMINISTRATION/HANDLING
Treatment of susceptible infections due to IV
S. aureus, S. epidermidis, group A beta-
hemolytic streptococci, S. pneumoniae, Reconstitution • Reconstitute each 1 g
E. coli, P. mirabilis, Klebsiella spp., H. with at least 10 mL Sterile Water for
influenzae, including biliary tract, bone Injection or 0.9% NaCl. • May further

underlined – top prescribed drug


ceFAZolin 207
dilute in 50–100 mL D5W or 0.9% Creatinine
NaCl (decreases incidence of thrombo- Clearance Dosage
phlebitis). 11–34 mL/min 50% usual dose q12h
Rate of administration • For IV 10 mL/min 50% usual dose q18–24h C
push, administer over 3–5 min (maxi- or less
mum concentration: 100 mg/ HD 500 mg–1 g q24h
PD 500 mg q12h
mL). • For intermittent IV infusion CRRT
(piggyback), infuse over 30–60 min CVVH Loading dose 2 g, then
(maximum concentration: 20 mg/ 1–2 g q12h
mL). CVVHD/CVVHDF Loading dose 2 g, then
Storage • Solution appears light yel- 1 g q8h or 2 g q12h
low to yellow in color. • Reconstituted
solution stable for 24 hrs at room tem- Dosage in Hepatic Impairment
perature or for 10 days if refriger- No dose adjustment.
ated. • IV infusion (piggyback) stable
for 48 hrs at room temperature or for 14 SIDE EFFECTS
days if refrigerated. Frequent: Discomfort with IM adminis-
IM tration, oral candidiasis (thrush), mild
• To minimize discomfort, inject deep diarrhea, mild abdominal cramping,
IM slowly. • Less painful if injected into vaginal candidiasis. Occasional: Nausea,
gluteus maximus rather than lateral as- serum sickness–like reaction (fever, joint
pect of thigh. pain; usually occurs after second course
of therapy and resolves after drug is dis-
IV INCOMPATIBILITIES continued). Rare: Allergic reaction (rash,
Amikacin (Amikin), amiodarone (Cor- pruritus, urticaria), thrombophlebitis
darone), HYDROmorphone (Dilaudid). (pain, redness, swelling at injection site).

IV COMPATIBILITIES ADVERSE EFFECTS/TOXIC


REACTIONS
Calcium gluconate, dexamethasone
(Decadron), diltiaZEM (Cardizem), Antibiotic-associated colitis, other super-
famotidine (Pepcid), heparin, insu- infections (abdominal cramps, severe
lin (regular), lidocaine, LORazepam watery diarrhea, fever) may result from
(Ativan), magnesium sulfate, me- altered bacterial balance in GI tract.
peridine (Demerol), metoclopramide Nephrotoxicity may occur, esp. in pts with
(Reglan), midazolam (Versed), mor- preexisting renal disease. Pts with history
phine, multivitamins, ondansetron of penicillin allergy are at increased risk
(Zofran), potassium chloride, propo- for developing severe hypersensitivity
fol (Diprivan). reaction (severe pruritus, angioedema,
bronchospasm, anaphylaxis).
INDICATIONS/ROUTES/DOSAGE
NURSING CONSIDERATIONS
Usual Dosage Range
IV, IM: ADULTS: 1–1.5 g q6–12h (usu- BASELINE ASSESSMENT
ally q8h). Maximum: 12 g/day. CHIL- Obtain CBC, renal function tests. Ques-
DREN OLDER THAN 1 MO: 25–100 mg/kg/ tion for history of allergies, particularly
day divided q6–8h. Maximum: 6 g/day. cephalosporins, penicillins.
NEONATES: 25 mg/kg/dose q8–12h.
INTERVENTION/EVALUATION
Dosage in Renal Impairment Evaluate IM site for induration and ten-
Dosing frequency is modified based on derness. Assess oral cavity for white
creatinine clearance. patches on mucous membranes, tongue

Canadian trade name Non-Crushable Drug High Alert drug


208 cefdinir
(thrush). Monitor daily pattern of bowel Primarily excreted in urine. Minimally re-
activity, stool consistency. Mild GI effects moved by hemodialysis. Half-life: 1–2
may be tolerable (increasing severity may hrs (increased in renal impairment).
C indicate onset of antibiotic-associated
colitis). Monitor I&O, renal function tests LIFESPAN CONSIDERATIONS
for nephrotoxicity. Be alert for superin- Pregnancy/Lactation: Crosses pla-
fection: fever, vomiting, diarrhea, anal/ centa. Not detected in breast milk. Chil-
genital pruritus, oral mucosal changes dren: Newborns, infants may have lower
(ulceration, pain, erythema). renal clearance. Elderly: Age-related
renal impairment may require decreased
PATIENT/FAMILY TEACHING
dosage or increased dosing interval.
• Discomfort may occur with IM
­injection. INTERACTIONS
DRUG: Antacids, iron preparations
may interfere with absorption. Probenecid
increases concentration. HERBAL: None
cefdinir significant. FOOD: None known. LAB VAL-
UES: May produce false-positive reaction
sef-di-neer for urine ketones. May increase serum alka-
line phosphatase, bilirubin, LDH, ALT, AST.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Third- AVAILABILITY (Rx)
generation cephalosporin. CLINI- Capsules: 300 mg. Powder for Oral
CAL: Antibiotic.
Suspension: 125 mg/5 mL, 250 mg/5 mL.

USES ADMINISTRATION/HANDLING
PO
Treatment of susceptible infections due to
• Give without regard to food. Give at
S. pyogenes, S. pneumoniae, H. influen-
least 2 hrs before or after antacids or
zae, H. parainfluenzae, M. catarrhalis,
iron supplements. • Twice-daily doses
including community-acquired pneumo-
should be given 12 hrs apart. • Shake
nia, acute exacerbation of chronic bron-
oral suspension well before administer-
chitis, acute maxillary sinusitis, pharyn-
ing. • Store mixed suspension at room
gitis, tonsillitis, uncomplicated skin/skin
temperature for 10 days.
structure infections, otitis media.
PRECAUTIONS INDICATIONS/ROUTES/DOSAGE
Usual Dosage Range
Contraindications: Hypersensitivity to
PO: ADULTS, ELDERLY: 300 mg q12h or
cefdinir. History of anaphylactic reaction
600 mg once daily. CHILDREN 6 MOS–12
to cephalosporins. Cautions: Hypersen-
YRS: 7 mg/kg q12h or 14 mg/kg once
sitivity to penicillins; renal impairment.
daily. Maximum: 600 mg/day.
ACTION Dosage in Renal Impairment
Binds to bacterial cell membranes, in- CrCl less than 30 mL/min: 300 mg/
hibits cell wall synthesis. Therapeutic day or 7 mg/kg as single daily dose. Maxi-
Effect: Bactericidal. mum: 300 mg. Hemodialysis pts:
300 mg or 7 mg/kg/dose every other day.
PHARMACOKINETICS Maximum: 300 mg.
Moderately absorbed from GI tract.
Protein binding: 60%–70%. Widely dis- Dosage in Hepatic Impairment
tributed. Not appreciably metabolized. No dose adjustment.

underlined – top prescribed drug


cefepime 209

SIDE EFFECTS
Frequent: Oral candidiasis, mild diar-
cefepime
rhea, mild abdominal cramping, vaginal
sef-e-peem C
candidiasis. Occasional: Nausea, serum
(Maxipime)
sickness–like reaction (fever, joint pain;
Do not confuse cefepime with
usually occurs after second course of
cefixime or cefTAZidime.
therapy and resolves after drug is discon-
tinued). Rare: Allergic reaction (rash, uCLASSIFICATION
pruritus, urticaria).
PHARMACOTHERAPEUTIC: Fourth-
ADVERSE EFFECTS/TOXIC generation cephalosporin. CLINI-
REACTIONS CAL: Antibiotic.
Antibiotic-associated colitis, other su-
perinfections (abdominal cramps, se- USES
vere watery diarrhea, fever) may result Susceptible infections due to aerobic
from altered bacterial balance in GI gram-negative organisms including P.
tract. Nephrotoxicity may occur, esp. in aeruginosa, gram-positive organisms in-
pts with preexisting renal disease. Pts cluding S. aureus. Treatment of empiric
with history of penicillin allergy are at febrile neutropenia, intra-abdominal in-
increased risk for developing a severe fections, skin/skin structure infections,
hypersensitivity reaction (severe pruri- UTIs, pneumonia. OFF-LABEL: Brain
tus, angioedema, bronchospasm, ana- abscess, malignant otitis externa, septic
phylaxis). lateral/cavernous sinus thrombus.
NURSING CONSIDERATIONS PRECAUTIONS
BASELINE ASSESSMENT Contraindications: History of anaphy-
Obtain CBC, renal function tests. Ques- lactic reaction to penicillins, hypersen-
tion for hypersensitivity to cefdinir or sitivity to cefepime, cephalosporins.
other cephalosporins, penicillins. Cautions: Renal impairment, history of
seizure disorder, GI disease (colitis),
INTERVENTION/EVALUATION elderly.
Observe for rash. Monitor daily pattern
of bowel activity, stool consistency. Mild ACTION
GI effects may be tolerable (increasing Binds to bacterial cell wall membranes,
severity may indicate onset of antibiotic- inhibits cell wall synthesis. Therapeutic
associated colitis). Be alert for superin- Effect: Bactericidal.
fection: fever, vomiting, diarrhea, anal/
genital pruritus, oral mucosal changes PHARMACOKINETICS
(ulceration, pain, erythema). Monitor Well absorbed after IM administration.
hematology reports. Protein binding: 20%. Widely distributed.
PATIENT/FAMILY TEACHING
Primarily excreted in urine. Removed
by hemodialysis. Half-life: 2–2.3 hrs
• Take antacids 2 hrs before or follow- (increased in renal impairment, elderly
ing medication. • Continue medication pts).
for full length of treatment; do not skip
doses. • Doses should be evenly LIFESPAN CONSIDERATIONS
spaced. • Report persistent severe di- Pregnancy/Lactation: Unknown if
arrhea, rash, muscle aches, fever, en- distributed in breast milk. Children: No
larged lymph nodes, joint pain. age-related precautions noted in pts
older than 2 mos. Elderly: Age-related

Canadian trade name Non-Crushable Drug High Alert drug


210 cefepime
renal impairment may require reduced ofloxacin (Floxin), ondansetron (Zo-
dosage or increased dosing interval. fran), vancomycin (Vancocin).

C INTERACTIONS IV COMPATIBILITIES
DRUG: Probenecid may increase con- Bumetanide (Bumex), calcium gluco-
centration. May increase aminogly- nate, furosemide (Lasix), HYDROmor-
coside concentration. HERBAL: None phone (Dilaudid), LORazepam (Ativan),
significant. FOOD: None known. LAB propofol (Diprivan).
VALUES: May increase serum BUN, al-
kaline phosphatase, bilirubin, LDH, ALT, INDICATIONS/ROUTES/DOSAGE
AST. May cause positive direct/indirect Usual Dosage Range
Coombs’ test. IV: ADULTS, ELDERLY: 1–2 g q8–12h. CHIL-
DREN: 50 mg/kg q8–12h not to exceed
AVAILABILITY (Rx) adult dosing. NEONATES: 30 mg/kg q12h
Injection, Powder for Reconstitution: 1 g, up to 50 mg/kg q8–12h.
2 g. Injection, Premix: 1 g (50 mL), 2 g
(100 mL). Dosage in Renal Impairment
Dosage and frequency are modified
ADMINISTRATION/HANDLING based on creatinine clearance and sever-
ity of infection.
IV
Creatinine Clearance Dosage
Reconstitution • Add 10 mL of dilu- 30–60 mL/min 500 mg q24h–2 g
ent for 1-g and 2-g vials. • Further di- q12h
lute with 50–100 mL 0.9% NaCl or D5W. 11–29 mL/min 500 mg–2 g q24h
Rate of administration • For inter- 10 mL/min or less 250 mg–1 g q24h
mittent IV infusion (piggyback), infuse Hemodialysis Initially, 1 g, then
0.5–1 g q24h or
over 30 min. For direct IV, administer 1–2 g q48–72h
over 5 min. Peritoneal dialysis Normal dose q48h
Storage • Solution is stable for 24 hrs Continuous renal re- Initially, 2 g, then 1
at room temperature, 7 days if refriger- placement therapy g q8h or 2 g q12h
ated.
IM Dosage in Hepatic Impairment
• Add 2.4 mL Sterile Water for Injection, No dose adjustment.
0.9% NaCl, or D5W to 1-g and 2-g vi-
als. • Inject into a large muscle mass SIDE EFFECTS
(e.g., upper gluteus maximus). Frequent: Discomfort with IM adminis-
tration, oral candidiasis (thrush), mild
IV INCOMPATIBILITIES diarrhea, mild abdominal cramping,
Acyclovir (Zovirax), amphotericin (Fun- vaginal candidiasis. Occasional: Nausea,
gizone), cimetidine (Tagamet), cipro- serum sickness–like reaction (fever, joint
floxacin (Cipro), CISplatin (Platinol), pain; usually occurs after second course
dacarbazine (DTIC), DAUNOrubicin of therapy and resolves after drug is dis-
(Cerubidine), diazePAM (Valium), di- continued). Rare: Allergic reaction (rash,
phenhydrAMINE (Benadryl), DOBUTa- pruritus, urticaria), thrombophlebitis
mine (Dobutrex), DOPamine (Intropin), (pain, redness, swelling at injection site).
DOXOrubicin (Adriamycin), droperidol
(Inapsine), famotidine (Pepcid), ganci- ADVERSE EFFECTS/TOXIC
clovir (Cytovene), haloperidol (Haldol), REACTIONS
magnesium, magnesium sulfate, manni- Antibiotic-associated colitis, other super-
tol, metoclopramide (Reglan), morphine, infections (abdominal cramps, severe

underlined – top prescribed drug


cefixime 211
watery diarrhea, fever) may result from USES
altered bacterial balance in GI tract. Treatment of susceptible infections due to
Nephrotoxicity may occur, esp. in pts with S. pneumoniae, S. pyogenes, M. catarrh-
preexisting renal disease. Pts with history alis, H. influenzae, E. coli, P. mirabilis, C
of penicillin allergy are at increased risk including otitis media, acute bronchitis,
for developing a severe hypersensitivity acute exacerbations of chronic bronchitis,
reaction (severe pruritus, angioedema, pharyngitis, tonsillitis, uncomplicated UTI.
bronchospasm, anaphylaxis).
PRECAUTIONS
NURSING CONSIDERATIONS
Contraindications: History of hypersen-
BASELINE ASSESSMENT sitivity/anaphylactic reaction to cefixime,
Obtain CBC, renal function tests. Ques- cephalosporins. Cautions: History of
tion for history of allergies, particularly penicillin allergy, renal impairment.
cephalosporins, penicillins.
ACTION
INTERVENTION/EVALUATION Binds to bacterial cell membranes, in-
Evaluate IM site for induration and ten- hibits cell wall synthesis. Therapeutic
derness. Assess oral cavity for white Effect: Bactericidal.
patches on mucous membranes, tongue
(thrush). Monitor daily pattern of bowel PHARMACOKINETICS
activity, stool consistency. Mild GI effects Moderately absorbed from GI tract. Protein
may be tolerable (increasing severity may binding: 65%–70%. Widely distributed.
indicate onset of antibiotic-associated Primarily excreted in urine. Minimally re-
colitis). Monitor I&O, CBC, renal func- moved by hemodialysis. Half-life: 3–4
tion tests for nephrotoxicity. Be alert hrs (increased in renal impairment).
for superinfection: fever, vomiting, diar-
rhea, anal/genital pruritus, oral mucosal LIFESPAN CONSIDERATIONS
changes (ulceration, pain, erythema). Pregnancy/Lactation: Not recom-
mended during labor and delivery. Un-
PATIENT/FAMILY TEACHING
known if distributed in breast milk. Chil-
• Discomfort may occur with IM injec- dren: Safety and efficacy not established
tion. • Continue therapy for full length in pts younger than 6 mos. Elderly: Age-
of treatment. • Doses should be evenly related renal impairment may require
spaced. • Report persistent diarrhea. dosage adjustment.
INTERACTIONS
DRUG: Probenecid may increase con-
cefixime centration. HERBAL: None significant.
FOOD: None known. LAB VALUES: May
sef-ix-eem increase serum BUN, alkaline phospha-
(Suprax) tase, bilirubin, creatinine, LDH, ALT,
Do not confuse cefixime with AST. May cause a positive direct/indirect
cefepime, or Suprax with Spo- Coombs’ test.
ranox or Surbex.
AVAILABILITY (Rx)
uCLASSIFICATION
Oral Suspension: 100 mg/5 mL, 200 mg/5
PHARMACOTHERAPEUTIC: Third- mL, 500 mg/5 mL. Capsules: 400 mg.
generation cephalosporin. CLINI- Tablets (Chewable): 100 mg, 200 mg.
CAL: Antibiotic.

Canadian trade name Non-Crushable Drug High Alert drug


212 cefotaxime

ADMINISTRATION/HANDLING for developing a severe hypersensitivity


PO reaction (severe pruritus, angioedema,
• Give without regard to food. • After bronchospasm, anaphylaxis).
C reconstitution, oral suspension is stable
NURSING CONSIDERATIONS
for 14 days at room temperature or re-
frigerated. • Shake oral suspension BASELINE ASSESSMENT
well before administering. Chewable tab- Obtain CBC, renal function tests. Ques-
lets must be chewed or crushed before tion for hypersensitivity to cefixime or
swallowing. other cephalosporins, penicillins.
INDICATIONS/ROUTES/DOSAGE INTERVENTION/EVALUATION
Usual Dosage Assess oral cavity for white patches on
PO: ADULTS, ELDERLY, CHILDREN 12 YRS mucous membranes, tongue (thrush).
AND OLDER WEIGHING MORE THAN 45 Monitor daily pattern of bowel activity,
KG: 400 mg/day as a single dose or in stool consistency. Mild GI effects may
2 divided doses. CHILDREN 6 MOS–12 YRS be tolerable (increasing severity may
WEIGHING 45 KG OR LESS: 8 mg/kg/day indicate onset of antibiotic-associated
as a single dose or in 2 divided doses. colitis). Monitor renal function tests for
Maximum: 400 mg. evidence of nephrotoxicity. Be alert for
superinfection: fever, vomiting, diar-
Dosage in Renal Impairment rhea, anal/genital pruritus, oral mucosal
Dosage is modified based on creatinine changes (ulceration, pain, erythema).
clearance.
Creatinine Clearance Dosage PATIENT/FAMILY TEACHING
21–60 mL/min 260 mg/day • Continue medication for full length of
20 mL/min or less 200 mg/day treatment; do not skip doses. • Doses
Hemodialysis 260 mg/day should be evenly spaced. • May cause
GI upset (may take with food or
Dosage in Hepatic Impairment milk). • Report persistent diarrhea.
No dose adjustment.
SIDE EFFECTS
Frequent: Oral candidiasis (thrush), cefotaxime
mild diarrhea, mild abdominal cramping,
vaginal candidiasis. Occasional: Nausea, sef-oh-tax-eem
serum sickness–like reaction (arthral- (Claforan )
gia, fever; usually occurs after second Do not confuse cefotaxime with
course of therapy and resolves after drug cefOXitin, ceftizoxime, or cefuro-
is discontinued). Rare: Allergic reaction xime, or Claforan with Claritin.
(rash, pruritus, urticaria). uCLASSIFICATION
ADVERSE EFFECTS/TOXIC PHARMACOTHERAPEUTIC: Third-
REACTIONS generation cephalosporin. CLINI-
Antibiotic-associated colitis, other super- CAL: Antibiotic.
infections (abdominal cramps, severe
watery diarrhea, fever) may result from USES
altered bacterial balance in GI tract.
Nephrotoxicity may occur, esp. in pts with Treatment of susceptible infections (active
preexisting renal disease. Pts with history vs. most gram-negative [not Pseudomo-
of penicillin allergy are at increased risk nas] and gram-positive cocci [not En-
terococcus]), including bone, joint, GU,
underlined – top prescribed drug
cefotaxime 213
gynecologic, intra-abdominal, lower respi- of 100 mg/mL. • May further dilute with
ratory tract, skin/skin structure infections; 50–100 mL 0.9% NaCl or D5W.
septicemia, meningitis, perioperative pro- Rate of administration • For IV
phylaxis. OFF-LABEL: Surgical prophylaxis. push, administer over 3–5 min. • For C
intermittent IV infusion (piggyback), in-
PRECAUTIONS fuse over 15–30 min.
Contraindications: History of hypersensi- Storage • Solution appears light yel-
tivity/anaphylactic reaction to cefotaxime, low to amber. • IV infusion (piggy-
cephalosporins. Cautions: History of back) is stable for 24 hrs at room tem-
penicillin allergy, colitis, renal impair- perature, 5 days if refrigerated. •
ment with CrCl less than 30 mL/min. Discard if precipitate forms.
ACTION IM
Binds to bacterial cell membranes, in- • Reconstitute with Sterile Water for In-
hibits cell wall synthesis. Therapeutic jection or Bacteriostatic Water for Injec-
Effect: Bactericidal. tion to provide a concentration of 230–
330 mg/mL. • To minimize discomfort,
PHARMACOKINETICS inject deep IM slowly. Less painful if in-
Widely distributed to CSF. Protein binding: jected into gluteus maximus than lateral
30%–50%. Partially metabolized in liver. aspect of thigh. For 2-g IM dose, give at 2
Primarily excreted in urine. Moderately separate sites.
removed by hemodialysis. Half-life: 1 hr
(increased in renal impairment). IV INCOMPATIBILITIES
Allopurinol (Aloprim), filgrastim (Ne-
LIFESPAN CONSIDERATIONS upogen), fluconazole (Diflucan), vanco-
Pregnancy/Lactation: Readily crosses mycin (Vancocin).
placenta. Distributed in breast milk. Chil-
dren: No age-related precautions noted.
IV COMPATIBILITIES
Elderly: Age-related renal impairment DiltiaZEM (Cardizem), famotidine (Pep-
may require dosage adjustment. cid), HYDROmorphone (Dilaudid), LO-
Razepam (Ativan), magnesium sulfate,
INTERACTIONS midazolam (Versed), morphine, propo-
DRUG: Probenecid may increase con- fol (Diprivan).
centration. HERBAL: None significant.
FOOD: None known. LAB VALUES: May
INDICATIONS/ROUTES/DOSAGE
cause positive direct/indirect Coombs’ test. Usual Dosage Range
May increase serum BUN, creatinine, ALT, IV, IM: ADULTS, ELDERLY, CHILDREN
AST, alkaline phosphatase. WEIGHING 50 KG OR MORE: Uncomplicated
infection: 1 g q12h. Moderate to severe
AVAILABILITY (Rx) infection: 1–2 g q8h. Life-threatening
Injection, Powder for Reconstitution: 1 g. infection: 2 g q4h. CHILDREN 1 MO–12
YRS WEIGHING LESS THAN 50 KG: Mild to
ADMINISTRATION/HANDLING moderate infection: 50–180 mg/kg/day
in divided doses q6–8h. Maximum:
IV
6 g/day. Severe infection: 200–225 mg/
Reconstitution • Reconstitute with 10 kg/day in divided doses q4–6h. Maxi-
mL Sterile Water for Injection or 0.9% mum: 12 g/day. NEONATES: 50 mg/kg/
NaCl to provide a maximum concentration dose q8–12h.

Canadian trade name Non-Crushable Drug High Alert drug


214 cefpodoxime
Dosage in Renal Impairment colitis). Monitor I&O, renal function tests
Creatinine Clearance Dosage Interval for nephrotoxicity. Be alert for superin-
10–50 mL/min 6–12 hrs fection: fever, vomiting, diarrhea, anal/
C Less than 10 mL/min 24 hrs genital pruritus, oral mucosal changes
Hemodialysis 1–2g q24h (ulceration, pain, erythema).
Peritoneal dialysis 1g q24h
CVVH 1–2 g q8–12h PATIENT/FAMILY TEACHING
CVVHD 1–2g q8h • Discomfort may occur with IM injec-
CVVHDF 1–2g q6–8h tion. • Doses should be evenly
spaced. • Continue antibiotic therapy
Dosage in Hepatic Impairment for full length of treatment.
No dose adjustment.
SIDE EFFECTS
Frequent: Discomfort with IM adminis-
cefpodoxime
tration, oral candidiasis (thrush), mild sef-poe-dox-eem
diarrhea, mild abdominal cramping,
vaginal candidiasis. Occasional: Nausea, uCLASSIFICATION
serum sickness–like reaction (fever, joint PHARMACOTHERAPEUTIC: Third-
pain; usually occurs after second course generation cephalosporin. CLINI-
of therapy and resolves after drug is dis- CAL: Antibiotic.
continued). Rare: Allergic reaction (rash,
pruritus, urticaria), thrombophlebitis
(pain, redness, swelling at injection site). USES
ADVERSE EFFECTS/TOXIC Treatment of susceptible infections due to
REACTIONS S. pneumoniae, S. pyogenes, S. aureus,
H. influenzae, M. catarrhalis, E. coli,
Antibiotic-associated colitis, other super- Proteus, Klebsiella spp., including acute
infections (abdominal cramps, severe maxillary sinusitis, chronic bronchitis,
watery diarrhea, fever) may result from community-acquired pneumonia, otitis
altered bacterial balance in GI tract. media, pharyngitis, tonsillitis, skin/skin
Nephrotoxicity may occur, esp. in pts with structure infections, UTIs.
preexisting renal disease. Pts with history
of penicillin allergy are at increased risk PRECAUTIONS
for developing a severe hypersensitivity Contraindications: History of hypersensi-
reaction (severe pruritus, angioedema, tivity/anaphylactic reaction to cefpodox-
bronchospasm, anaphylaxis). ime, cephalosporins. Cautions: Renal
NURSING CONSIDERATIONS impairment, history of penicillin allergy.

BASELINE ASSESSMENT ACTION


Question for history of allergies, particu- Binds to bacterial cell membranes, in-
larly cephalosporins, penicillins. hibits cell wall synthesis. Therapeutic
Effect: Bactericidal.
INTERVENTION/EVALUATION
Check IM injection sites for induration, PHARMACOKINETICS
tenderness. Assess oral cavity for white Well absorbed from GI tract (food increases
patches on mucous membranes, tongue absorption). Protein binding: 18%–23%.
(thrush). Monitor daily pattern of bowel Widely distributed. Primarily excreted un-
activity, stool consistency. Mild GI effects changed in urine. Partially removed by he-
may be tolerable (increasing severity may modialysis. Half-life: 2.3 hrs (increased
indicate onset of antibiotic-associated in renal impairment, elderly pts).
underlined – top prescribed drug
cefpodoxime 215

LIFESPAN CONSIDERATIONS vaginal candidiasis. Occasional: Nausea,


Pregnancy/Lactation: Readily crosses serum sickness–like reaction (fever,
placenta. Distributed in breast milk. joint pain; usually occurs after second
Children: Safety and efficacy not es-
course of therapy and resolves after drug C
tablished in pts younger than 6 mos. is discontinued). Rare: Allergic reaction
Elderly: Age-related renal impairment
(pruritus, rash, urticaria).
may require dosage adjustment. ADVERSE EFFECTS/TOXIC
INTERACTIONS REACTIONS
DRUG: High doses of antacids contain- Antibiotic-associated colitis, other su-
ing aluminum, H2 antagonists (e.g., perinfections (abdominal cramps, se-
famotidine, ranitidine) may decrease vere watery diarrhea, fever) may result
absorption. Probenecid may increase from altered bacterial balance in GI
concentration. HERBAL: None signifi- tract. Nephrotoxicity may occur, esp. in
cant. FOOD: Food enhances absorption. pts with preexisting renal disease. Pts
LAB VALUES: May increase serum BUN,
with history of penicillin allergy are at
alkaline phosphatase, bilirubin, creati- increased risk for developing a severe
nine, LDH, ALT, AST. May cause positive hypersensitivity reaction (severe pruri-
direct/indirect Coombs’ test. tus, angioedema, bronchospasm, ana-
phylaxis).
AVAILABILITY (Rx)
NURSING CONSIDERATIONS
Oral Suspension: 50 mg/5 mL, 100 mg/5
mL. Tablets: 100 mg, 200 mg. BASELINE ASSESSMENT
Obtain CBC, renal function tests. Ques-
ADMINISTRATION/HANDLING tion for history of allergies, particularly
PO cephalosporins, penicillins.
• Administer tablet with food (enhances
absorption). • Administer suspension INTERVENTION/EVALUATION
without regard to food. • After recon- Assess oral cavity for white patches on
stitution, oral suspension is stable for 14 mucous membranes, tongue (thrush).
days if refrigerated. Monitor daily pattern of bowel activity,
stool consistency. Mild GI effects may
INDICATIONS/ROUTES/DOSAGE be tolerable (increasing severity may
Usual Dosage Range indicate onset of antibiotic-associated
PO: ADULTS, ELDERLY, CHILDREN OLDER colitis). Monitor I&O, renal func-
THAN 12 YRS: 100–400 mg q12h. CHIL- tion tests for nephrotoxicity. Be alert
DREN 2 MOS–12 YRS: 10 mg/kg/day in 2 for superinfection: fever, vomiting,
divided doses. Maximum: 200 mg/dose. diarrhea, anal/genital pruritus, oral
mucosal changes (ulceration, pain,
Dosage in Renal Impairment erythema).
For pts with CrCl less than 30 mL/min,
usual dose is given q24h. For pts on he- PATIENT/FAMILY TEACHING
modialysis, usual dose is given 3 times/ • Doses should be evenly spaced. •
wk after dialysis. Shake oral suspension well before us-
ing. • Take tablets with food (enhances
Dosage in Hepatic Impairment absorption). • Continue antibiotic ther-
No dose adjustment. apy for full length of treatment. • Refrig-
erate oral suspension. • Report persis-
SIDE EFFECTS tent diarrhea.
Frequent: Oral candidiasis (thrush),
mild diarrhea, mild abdominal cramping,

Canadian trade name Non-Crushable Drug High Alert drug


216 cefprozil
Elderly: Age-related renal impairment
cefprozil may require dosage adjustment.

C sef-proe-zil INTERACTIONS
(Apo-Cefprozil , Cefzil ) DRUG: Probenecid may increase con-
Do not confuse cefprozil with centration. HERBAL: None significant.
ceFAZolin, or Cefzil with Cefol, FOOD: None known. LAB VALUES: May
Ceftin, or Kefzol. cause positive direct/indirect Coombs’
test. May increase serum BUN, creatinine,
uCLASSIFICATION
alkaline phosphatase, ALT, AST.
PHARMACOTHERAPEUTIC: Second-
generation cephalosporin. CLINI- AVAILABILITY (Rx)
CAL: Antibiotic. Oral Suspension: 125 mg/5 mL, 250
mg/5 mL. Tablets: 250 mg, 500 mg.
USES ADMINISTRATION/HANDLING
Treatment of susceptible infections due PO
to S. pneumoniae, S. pyogenes, S. au- • Give without regard to food; if GI upset
reus, H. influenzae, M. catarrhalis, occurs, give with food, milk. • After
including pharyngitis, tonsillitis, otitis reconstitution, oral suspension is stable
media, secondary bacterial infection of for 14 days if refrigerated. • Shake oral
acute bronchitis, acute bacterial exac- suspension well before using.
erbation of chronic bronchitis, uncom-
plicated skin/skin structure infections, INDICATIONS/ROUTES/DOSAGE
acute sinusitis. Usual Dosage Range
PO: ADULTS, ELDERLY, CHILDREN OLDER
PRECAUTIONS
THAN 12 YRS: 250–500 mg q12h or 500
Contraindications: History of hypersen- mg q24h. CHILDREN OLDER THAN 6 MOS–12
sitivity/anaphylactic reaction to cefpro- YRS: 7.5–15 mg/kg/day in 2 divided
zil, cephalosporins. Cautions: Severe doses. Maximum: 500 mg/dose. Do not
renal impairment, history of penicillin exceed adult dose.
allergy.
Dosage in Renal Impairment
ACTION CrCl less than 30 mL/min: 50% of
Binds to bacterial cell membranes, in- usual dose at usual interval. Hemodialy-
hibits cell wall synthesis. Therapeutic sis: Administer dose after completion of
Effect: Bactericidal. dialysis.
PHARMACOKINETICS Dosage in Hepatic Impairment
Well absorbed from GI tract. Protein No dose adjustment.
binding: 36%–45%. Widely distributed.
Primarily excreted in urine. Moderately SIDE EFFECTS
removed by hemodialysis. Half-life: 1.3 Frequent: Oral candidiasis (thrush),
hrs (increased in renal impairment). mild diarrhea, mild abdominal cramping,
vaginal candidiasis. Occasional: Nausea,
LIFESPAN CONSIDERATIONS serum sickness–like reaction (fever,
Pregnancy/Lactation: Readily crosses joint pain; usually occurs after second
placenta. Distributed in breast milk. course of therapy and resolves after drug
Children: Safety and efficacy not es- is discontinued). Rare: Allergic reaction
tablished in pts younger than 6 mos. (pruritus, rash, urticaria).

underlined – top prescribed drug


ceftaroline 217

ADVERSE EFFECTS/TOXIC USES


REACTIONS Treatment of susceptible infections due
Antibiotic-associated colitis, other super- to gram-positive and gram-negative
infections (abdominal cramps, severe organisms, including S. pneumoniae, C
watery diarrhea, fever) may result from S. aureus (methicillin-susceptible
altered bacterial balance in GI tract. only), H. influenzae, Klebsiella
Nephrotoxicity may occur, esp. in pts with pneumoniae, E. coli, including acute
preexisting renal disease. Pts with history bacterial skin and skin structure infec-
of penicillin allergy are at increased risk tions, community-acquired bacterial
for developing a severe hypersensitivity pneumonia.
reaction (severe pruritus, angioedema,
bronchospasm, anaphylaxis). PRECAUTIONS
Contraindications: History of hypersen-
NURSING CONSIDERATIONS sitivity/anaphylactic reaction to ceftaro-
BASELINE ASSESSMENT line, cephalosporins. Cautions: History
of allergy to penicillin, severe renal im-
Obtain CBC, renal function tests. Ques- pairment with CrCl less than 50 mL/min,
tion for history of allergies, particularly elderly.
cephalosporins, penicillins.
INTERVENTION/EVALUATION ACTION
Assess oral cavity for evidence of sto- Binds to bacterial cell membranes, in-
matitis. Monitor daily pattern of bowel hibits cell wall synthesis. Therapeutic
activity, stool consistency. Mild GI ef- Effect: Bactericidal.
fects may be tolerable (but increasing PHARMACOKINETICS
severity may indicate onset of antibiotic-
associated colitis). Monitor I&O, renal Protein binding: 20%. Widely distributed
function tests for nephrotoxicity. Be in plasma. Not metabolized. Primarily
alert for superinfection: fever, vomit- excreted in urine. Hemodialyzable. Half-
ing, diarrhea, anal/genital pruritus, oral life: 1.6 hrs (increased in renal impair-
mucosal changes (ulceration, pain, ery- ment).
thema). LIFESPAN CONSIDERATIONS
PATIENT/FAMILY TEACHING Pregnancy/Lactation: Unknown if dis-
• Doses should be evenly spaced. • tributed in breast milk. Children: Safety
Continue antibiotic therapy for full length and efficacy not established in pts younger
of treatment. • May cause GI upset than 18 yrs. Elderly: Age-related renal
(may take with food or milk). • Report impairment may require dose adjustment.
persistent diarrhea.
INTERACTIONS
DRUG: Probenecid may increase
concentration. HERBAL: None signifi-
ceftaroline cant. FOOD: None known. LAB VALUES:
May cause positive direct/indirect
sef-tar-o-leen Coombs’ test. May increase serum
(Teflaro) BUN, creatinine. May decrease serum
potassium.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Fifth- AVAILABILITY (Rx)
generation cephalosporin. CLINI- Injection, Powder for Reconstitution:
CAL: Antibiotic. 400-mg, 600-mg single-use vial.

Canadian trade name Non-Crushable Drug High Alert drug


218 cefTAZidime

ADMINISTRATION/HANDLING ADVERSE EFFECTS/TOXIC


b ALERT c Give by intermittent IV infu- REACTIONS
sion (piggyback). Do not give IV push. Antibiotic-associated colitis, other superin-
C Reconstitution • Reconstitute either fections (abdominal cramps, severe watery
400-mg or 600-mg vial with 20 mL Ster- diarrhea, fever) may result from altered
ile Water for Injection. • Mix gently to bacterial balance in GI tract. Nephrotoxic-
dissolve powder. • Further dilute with ity may occur, esp. with preexisting renal
50–250 mL D5W, 0.9% NaCl. disease. Pts with history of penicillin allergy
Rate of administration • Infuse over are at increased risk for developing a severe
5–60 min. hypersensitivity reaction (severe pruritus,
Storage • Discard if particulate is pres- angioedema, bronchospasm, anaphylaxis).
ent. • Following reconstitution, solution
should appear clear, light to dark yel- NURSING CONSIDERATIONS
low. • Solution is stable for 6 hrs at room BASELINE ASSESSMENT
temperature or 24 hrs if refrigerated.
Obtain CBC, renal function tests. Question
IV INCOMPATIBILITIES for hypersensitivity to other cephalospo-
Fluconazole (Diflucan), vancomycin rins, penicillins. For pts on hemodialysis,
(Vancocin). administer medication after dialysis.
INTERVENTION/EVALUATION
IV COMPATIBILITIES
Assess oral cavity for white patches on
Famotidine (Pepcid), HYDROmorphone mucous membranes, tongue (thrush).
(Dilaudid), LORazepam (Ativan), mag- Monitor daily pattern of bowel activity, stool
nesium sulfate, midazolam (Versed), consistency. Mild GI effects may be toler-
morphine, propofol (Diprivan). able, but increasing severity may indicate
INDICATIONS/ROUTES/DOSAGE onset of antibiotic-associated colitis. Moni-
tor I&O, renal function tests for evidence of
Usual Dosage nephrotoxicity. Be alert for superinfection:
IV: ADULTS, ELDERLY: 600 mg q12h. fever, vomiting, severe genital/anal pruritus,
CHILDREN 2–18 YRS (WEIGHING MORE THAN moderate to severe diarrhea, oral mucosal
33 KG): 400 mg q8h or 600 mg q12h. changes (ulceration, pain, erythema).
(WEIGHING 33 KG OR LESS): 12 mg/kg q8h.
CHILDREN 2 MOS TO LESS THAN 2 YRS: 8 PATIENT/FAMILY TEACHING
mg/kg q8h. • Continue medication for full length of
treatment. • Doses should be evenly
Dosage in Renal Impairment spaced.
Creatinine
Clearance Dosage
30–50 mL/min
15–29 mL/min
400 mg q12h
300 mg q12h
cefTAZidime
End-stage renal 200 mg every 12 hrs
disease, hemodi- (give after dialy- sef-taz-i-deem
alysis sis) (Fortaz, Tazicef)
Do not confuse cefTAZidime
Dosage in Hepatic Impairment with ceFAZolin, cefepime, or
No dose adjustment. cefTRIAXone.
SIDE EFFECTS uCLASSIFICATION
Occasional (5%–4%): Diarrhea, nausea. PHARMACOTHERAPEUTIC: Third-
Rare (3%–2%): Allergic reaction (rash, generation cephalosporin. CLINI-
pruritus, urticaria), phlebitis. CAL: Antibiotic.

underlined – top prescribed drug


cefTAZidime 219

USES ADMINISTRATION/HANDLING
Treatment of susceptible infections due b ALERT c Give by IM injection, direct
to gram-negative organisms (including IV injection (IV push), or intermittent IV
Pseudomonas and Enterobacteriaceae), infusion (piggyback). C
including bone, joint, CNS (including men- IV
ingitis), gynecologic, intra-abdominal,
lower respiratory tract, skin/skin structure Reconstitution • Add 10 mL Sterile
infections; UTI, septicemia. Treatment of Water for Injection to each 1 g to provide
CNS infections due to H. influenzae, N. concentration of 90 mg/mL. • May fur-
meningitidis, including meningitis. OFF- ther dilute with 50–100 mL 0.9% NaCl,
LABEL: Bacterial endophthalmitis. D5W, or other compatible diluent.
Rate of administration • For IV
PRECAUTIONS push, administer over 3–5 min (maxi-
Contraindications: History of hypersen- mum concentration: 180 mg/
sitivity/anaphylactic reaction to cefTAZi- mL). • For intermittent IV infusion
dime, cephalosporins. Cautions: Severe (piggyback), infuse over 15–30 min.
renal impairment, history of penicillin Storage • Solution appears light yellow
allergy, seizure disorder. to amber, tends to darken (color change
does not indicate loss of potency). • IV
ACTION infusion (piggyback) stable for 12 hrs at
Binds to bacterial cell membranes, in- room temperature or 3 days if refriger-
hibits cell wall synthesis. Therapeutic ated. • Discard if precipitate forms.
Effect: Bactericidal.
IM
PHARMACOKINETICS Reconstitution • Add 1.5 mL Sterile
Widely distributed, including to CSF. Water for Injection or lidocaine 1% to
Protein binding: 5%–17%. Primarily ex- 500-mg vial or 3 mL to 1-g vial to provide
creted in urine. Removed by hemodialy- a concentration of 280 mg/mL. • To
sis. Half-life: 2 hrs (increased in renal minimize discomfort, inject deep IM
impairment). slowly. Less painful if injected into glu-
teus maximus than lateral aspect of thigh.
LIFESPAN CONSIDERATIONS
IV INCOMPATIBILITIES
Pregnancy/Lactation: Readily crosses
placenta. Distributed in breast milk. Chil- Amphotericin B complex (Abelcet, Am-
dren: No age-related precautions noted. Bisome, Amphotec), fluconazole (Diflu-
Elderly: Age-related renal impairment can), IDArubicin, midazolam (Versed),
may require dosage adjustment. vancomycin (Vancocin).

INTERACTIONS IV COMPATIBILITIES
DRUG: Probenecid may increase concen- DiltiaZEM (Cardizem), famotidine (Pep-
tration/effect. HERBAL: None significant. cid), heparin, HYDROmorphone (Dilau-
FOOD: None known. LAB VALUES: May did), lipids, morphine, propofol (Diprivan).
increase serum BUN, alkaline phosphatase, INDICATIONS/ROUTES/DOSAGE
creatinine, LDH, ALT, AST. May cause posi-
tive direct/indirect Coombs’ test. Usual Dosage Range
IV, IM: ADULTS, ELDERLY: 500 mg–2 g
AVAILABILITY (Rx) q8–12h.
Injection, Powder for Reconstitution: (For- IV: CHILDREN 1 MO–12 YRS: Mild to mod-
taz, Tazicef): 500 mg, 1 g, 2 g. Injection, erate infection:90–150 mg/kg/day in
Premix: 1 g/50 mL. divided doses q8h. Maximum: 3 g/
day. Severe infection: 200 mg/kg/day in

Canadian trade name Non-Crushable Drug High Alert drug


220 cefTAZidime/avibactam
divided doses q8h. Maximum: 6 g/ NURSING CONSIDERATIONS
day. NEONATES 0–4 WKS: 50 mg/kg/dose
q8–12h. BASELINE ASSESSMENT
C Obtain CBC, renal function tests. Ques-
Dosage in Renal Impairment tion for history of allergies, particularly
Dosage and frequency are modified cephalosporins, penicillins.
based on creatinine clearance and sever-
ity of infection. INTERVENTION/EVALUATION
Creatinine Evaluate IV site for phlebitis (heat, pain,
Clearance Dosage red streaking over vein). Assess IM in-
31–50 mL/min 1g q12h jection sites for induration, tenderness.
16–30 mL/min 1g q24h Check oral cavity for white patches on
6–15 mL/min 500 mg q24h mucous membranes, tongue (thrush).
Less than 6 mL/min 500 mg q48h Monitor daily pattern of bowel activity,
Hemodialysis 0.5–1 g q24h or 1–2
stool consistency. Mild GI effects may
g q48–72h (give
post hemodialysis be tolerable (increasing severity may
on dialysis days) indicate onset of antibiotic-associated
Peritoneal dialysis Initially, 1 g, then colitis). Monitor I&O, renal function tests
0.5 g q24h for nephrotoxicity. Be alert for superin-
Continuous renal re- Initially, 2 g, then 1 fection: fever, vomiting, diarrhea, anal/
placement therapy g q8h or 2 g q12h genital pruritus, oral mucosal changes
(ulceration, pain, erythema).
Dosage in Hepatic Impairment PATIENT/FAMILY TEACHING
No dose adjustment.
• Discomfort may occur with IM injec-
SIDE EFFECTS tion. • Doses should be evenly
spaced. • Continue antibiotic therapy
Frequent: Discomfort with IM adminis-
for full length of treatment.
tration, oral candidiasis (thrush), mild
diarrhea, mild abdominal cramping,
vaginal candidiasis. Occasional: Nau-
sea, serum sickness–like reaction (fever,
cefTAZidime/
joint pain; usually occurs after second avibactam
course of therapy and resolves after drug
is discontinued). Rare: Allergic reaction sef-taz-i-deem/a-vi-bak-tam
(pruritus, rash, urticaria), thrombophle- (Avycaz)
bitis (pain, redness, swelling at injection Do not confuse cefTAZidime
site). with ceFAZolin or cefepime, or
avibactam with sulbactam or
ADVERSE EFFECTS/TOXIC tazobactam.
REACTIONS
Antibiotic-associated colitis, other su- uCLASSIFICATION
perinfections (abdominal cramps, se- PHARMACOTHERAPEUTIC: Cepha-
vere watery diarrhea, fever) may result losporin/beta-lactamase inhibitor.
from altered bacterial balance in GI CLINICAL: Antibacterial.
tract. Nephrotoxicity may occur, esp. in
pts with preexisting renal disease. Pts
with history of penicillin allergy are at USES
increased risk for developing a severe Used in combination with metroNI-
hypersensitivity reaction (severe pruri- DAZOLE for treatment of complicated
tus, angioedema, bronchospasm, ana- intra-abdominal infections caused by the
phylaxis). following susceptible microorganisms:
underlined – top prescribed drug
cefTAZidime/avibactam 221
E. cloacae, E. coli, K. pneumoniae, K. e­fficacy not established. Elderly: May
oxytoca, P. mirabilis, P. stuartii, and P. have increased risk of adverse effects
aeruginosa in adults and pediatric pts 3 (due to renal impairment).
mos and older. Treatment of complicated C
urinary tract infections, including pyelone- INTERACTIONS
phritis, caused by the following susceptible DRUG: May decrease therapeutic effect
microorganisms: C. freundii, C. koseri, E. of BCG (intravesical). HERBAL: None
aerogenes, E. cloacae, E. coli, K. pneu- significant. FOOD: None known. LAB VAL-
moniae, Proteus spp., and P. aeruginosa UES: May increase serum alkaline phospha-
in adults and pediatric pts 3 mos and older. tase, ALT, GGT, LDH. May decrease platelets,
Treatment of hospital-acquired bacterial eosinophils, leukocytes, lymphocytes, serum
pneumonia and ventilator-associated bac- potassium. May result in positive Coombs’
terial pneumonia (HAP/VAP) caused by the test or false-positive elevated urine glucose.
following susceptible microorganisms: K.
pneumoniae, E. cloacae, E. coli, Serra- AVAILABILITY (Rx)
tia marcescens, P. mirabilis, P. aerugi- b ALERT c CefTAZidime/avibactam is a
nosa, and Haemophilus influenzae. combination product.
Injection, Powder for Reconstitution: 2
PRECAUTIONS gm cefTAZidime/0.5 gm avibactam.
Contraindications: Hypersensitivity to avi- ADMINISTRATION/HANDLING
bactam-containing products, cefTAZidime,
cephalosporins. Cautions: History of renal IV
impairment, seizure disorder, encephalop- Reconstitution • Reconstitute vial with
athy, recent C. difficile (C-diff) infection or 10 mL of one of the following solutions:
antibiotic-associated colitis. Hypersensitiv- 0.9% NaCl, Sterile Water for Injection, or
ity to penicillins, other beta-lactams. 5% Dextrose Injection. • Shake gently
ACTION until powder is completely dissolved. • Vi-
sually inspect for particulate matter or dis-
Inhibits cell wall synthesis by binding to coloration. Solution should appear clear to
bacterial cell membrane. Bacterial ac- slightly yellow in color. • Final concentra-
tion of cefTAZidime is mediated through tion of vial will equal approx. 0.167 g/mL of
binding to essential penicillin-binding cefTAZidime and 0.042 g/mL of avibac-
proteins. Avibactam inactivates some beta- tam. • Further dilute with 50 mL to 250
lactamases and protects cefTAZidime from mL 0.9% NaCl or 5% Dextrose Injection.
degradation by certain beta-lactamases. Rate of administration • Infuse over
Therapeutic Effect: Bactericidal. 2 hrs.
Storage • Diluted solution may be
PHARMACOKINETICS
stored at room temperature up to 12 hrs
Widely distributed. Excreted unchanged as or refrigerated up to 24 hrs. • Infuse
parent drug; not significantly metabolized within 12 hrs once removed from refrig-
in liver. Protein binding: less than 10%. Re- erator. • Do not freeze.
moved extensively by hemodialysis (55% of
dose). Eliminated in urine (80%–90% un- INDICATIONS/ROUTES/DOSAGE
changed). Half-life: 2.7 hrs (dependent Complicated Intra-Abdominal Infections
on dose and severity of renal impairment). IV: ADULTS, ELDERLY: 2.5 g (cefTAZidime
2 g/avibactam 0.5 g) q8h for 5–14 days
LIFESPAN CONSIDERATIONS (in combination with metroNIDAZOLE).
Pregnancy/Lactation: CefTAZidime is INFANTS 6 MOS AND OLDER, CHILDREN, AD-
excreted in breast milk in low concentra- OLESCENTS YOUNGER THAN 18 YRS: 50 mg
tions. Unknown if avibactam is excreted cefTAZidime/kg/dose q8h; Maximum:
in breast milk. Children: Safety and 2g cefTAZidime/dose. INFANTS 3 MOS TO
Canadian trade name Non-Crushable Drug High Alert drug
222 cefTAZidime/avibactam
LESS THAN 6 MOS: 40 mg cefTAZidime/kg/ neutropenia, thrombocytopenia were re-
dose q8h. ported. Hypersensitivity reactions, includ-
ing anaphylaxis or severe skin reactions,
C Complicated Urinary Tract Infections have been reported in pts treated with
Including Pyelonephritis beta-lactam antibacterial drugs. C. dif-
IV: ADULTS, ELDERLY: 2.5 g (2 g cefTAZi- ficile (C-diff)–associated diarrhea, with
dime/0.5 g avibactam) q8h for 7–14 days. severity ranging from mild diarrhea to
INFANTS 6 MOS AND OLDER, CHILDREN, ADO- fatal colitis, was reported. C-diff infection
LESCENTS YOUNGER THAN 18 YRS: 50 mg may occur more than 2 mos after treat-
cefTAZidime/kg/dose q8h. Maximum: 2 ment completion. Central nervous system
g cefTAZidime/dose. INFANTS 3 MOS TO reactions including asterixis, coma, en-
LESS THAN 6 MOS: 40 mg cefTAZidime/kg/ cephalopathy, neuromuscular excitability,
dose q8h. myoclonus, nonconvulsive status epilepti-
HAP/VAP cus, seizures have been reported in pts re-
IV: ADULTS, ELDERLY: 2.5 g (2 g cefTAZi- ceiving cefTAZidime, esp. in pts with renal
dime/0.5 g avibactam) q8h for 7–14 days. impairment. May increase risk of develop-
ment of drug-resistant bacteria when used
Dosage in Renal Impairment in the absence of a proven or strongly
Note: Infuse after hemodialysis on suspected bacterial infection. Skin and
hemodialysis days. Dosage is modified subcutaneous tissue disorders such as
based on creatinine clearance. angioedema, erythema multiforme, pru-
Creatinine ritus, Stevens-Johnson syndrome, toxic
Clearance Dosage epidermal necrolysis were reported in
Greater than 50 2.5 g (2 g/0.5 g) q8h pts receiving cefTAZidime. Other reported
mL/min adverse effects, including infusion site in-
31–50 mL/min 1.25 g (1 g/0.25 g) q8h flammation/hematoma/thrombosis, jaun-
16–30 mL/min 0.94 g (0.75 g/0.19 g) dice, candidiasis, dysgeusia, paresthesia,
q12h tubulointerstitial nephritis, vaginal inflam-
6–15 mL/min 0.94 g (0.75 g/0.19 g) mation, occur rarely.
q24h
Less than or equal 0.94 g (0.75 g/0.19 g) NURSING CONSIDERATIONS
to 5 mL/min q48h
BASELINE ASSESSMENT
Dosage in Hepatic Impairment
No dose adjustment. Obtain baseline CBC, BUN, serum creati-
nine, potassium; CrCl, GFR, LFT; bacterial
SIDE EFFECTS culture and sensitivity; vital signs. Ques-
Occasional (14%–5%): Vomiting, nausea, tion history of recent C. difficile infec-
abdominal pain, anxiety, rash. Rare (4%– tion, renal impairment, seizure disorder;
2%): Constipation, dizziness.
hypersensitivity reaction to beta-lactams,
carbapenem, cephalosporins, PCN. As-
ADVERSE EFFECTS/TOXIC sess skin for wounds; assess hydration
REACTIONS status. Question pt’s usual stool charac-
May cause worsening of renal function or teristics (color, frequency, consistency).
acute renal failure in pts with renal im- INTERVENTION/EVALUATION
pairment. Clinical cure rates were lower Monitor CBC, BMP, renal function periodi-
in pts with CrCl 30–50 mL/min compared cally. For pts with changing renal function,
with those with CrCl greater than 50 mL/ monitor renal function test daily and adjust
min, and in pts receiving metroNIDAZOLE dose accordingly. Diligently monitor I&Os.
combination therapy. Blood and lymphatic Observe daily pattern of bowel activity, stool
disorders such as agranulocytosis, hemo- consistency (increased severity may indi-
lytic anemia, leukopenia, lymphocytosis, cate antibiotic-associated colitis). If fre-
underlined – top prescribed drug
ceftolozane/tazobactam 223
quent diarrhea occurs, obtain C. difficile intra-abdominal infections caused by
toxin screen and initiate isolation precau- the following susceptible gram-negative
tions until test result confirmed; manage and gram-positive microorganisms: B.
proper fluids levels/PO intake, electrolyte fragilis, E. cloacae, E. coli, K. oxytoca, C
levels, protein intake. Antibacterial drugs K. pneumoniae, P. mirabilis, P. aerugi-
that are not directed against C. difficile nosa, S. anginosus, S. constellatus, and
infection may need to be discontinued. S. salivarius in pts 18 yrs or older. Treat-
Report any sign of hypersensitivity reaction. ment of complicated urinary tract infec-
tions, including pyelonephritis, caused
PATIENT/FAMILY TEACHING
by the following susceptible gram-neg-
• It is essential to complete drug therapy ative microorganisms: E. coli, K. pneu-
despite symptom improvement. Early dis- moniae, P. mirabilis, and P. aeruginosa
continuation may result in antibacterial in pts 18 yrs or older. Treatment of hos-
resistance or increased risk of recurrent pital-acquired pneumonia and ventilator-
infection. • Report any episodes of di- associated bacterial pneumonia in pts 18
arrhea, esp. in the mos following treat- yrs and older caused by E. cloacae, E.
ment completion. Frequent diarrhea, fe- coli, Haemophilus influenzae, K. oxy-
ver, abdominal pain, blood-streaked stool toca, K. pneumoniae, P. mirabilis, P.
may indicate infectious diarrhea and may aeruginosa, and Serratia marcescens.
be contagious to others. • Report ab-
dominal pain, black/tarry stools, bruis- PRECAUTIONS
ing, yellowing of skin or eyes; dark urine, Contraindications: Hypersensitivity to
decreased urine output; skin problems ceftolozane/tazobactam, piperacillin/
such as development of sores, rash, skin tazobactam, or other beta-lactams. Cau-
bubbling/necrosis. • Drink plenty of tions: History of atrial fibrillation, elec-
fluids. • Report any nervous system trolyte imbalance–associated arrhyth-
changes such as anxiety, confusion, hal- mias, recent C. difficile (C-diff) infection
lucinations, muscle jerking, or seizure- or antibiotic-associated colitis, renal/
like activity. • Severe allergic reactions hepatic impairment, seizure disorder;
such as hives, palpitations, shortness of prior hypersensitivity to penicillins, other
breath, rash, tongue-swelling may occur. cephalosporins.
ACTION
ceftolozane/ Inhibits cell wall synthesis by binding to
tazobactam bacterial cell membrane. Bacterial ac-
tion of ceftolozane is mediated through
binding to essential penicillin-binding
cef-tol-oh-zane/tay-zoe-bak-tam proteins. Tazobactam inactivates certain
(Zerbaxa) beta-lactamases and binds to certain
Do not confuse ceftolozane with chromosomal and plasmid-mediated
cefTAZidime, or tazobactam bacterial beta-lactamases. Therapeutic
with avibactam or sulbactam. Effect: Bactericidal.
uCLASSIFICATION
PHARMACOKINETICS
PHARMACOTHERAPEUTIC: Cepha- Widely distributed. Excreted unchanged
losporin/beta-lactamase inhibitor. as parent drug; not significantly metabo-
CLINICAL: Antibacterial.
lized in liver. Protein binding: 16%–30%.
Eliminated in urine (95% unchanged).
USES Removed extensively by hemodialysis.
Half-life: 2.7 hrs (dependent on dose
Used in combination with metroNI-
and severity of renal impairment).
DAZOLE for treatment of complicated
Canadian trade name Non-Crushable Drug High Alert drug
224 ceftolozane/tazobactam

LIFESPAN CONSIDERATIONS for 1 hr prior to transfer to diluent


Pregnancy/Lactation: Unknown if dis- bag. • May refrigerate diluted solu-
tributed in breast milk. Children: Safety tion up to 7 days or store at room
C temperature up to 24 hrs. • Do not
and efficacy not established. Elderly: May
have increased risk of adverse effects (due freeze.
to renal impairment). INDICATIONS/ROUTES/DOSAGE
INTERACTIONS Complicated Intra-Abdominal Infections
IV: ADULTS, ELDERLY: 1.5 g (ceftolozane
DRUG: Probenecid may increase con-
centration/effect. FOOD: None known. 1 g/tazobactam 0.5 g) q8h for 4–14
LAB VALUES: May increase serum alka-
days (in combination with metroNIDA-
line phosphatase, ALT, AST, GGT. May de- ZOLE).
crease Hgb, Hct, platelets; serum potas- Complicated Urinary Tract Infections
sium, magnesium, phosphate. May result Including Pyelonephritis
in positive Coombs’ test. IV: ADULTS, ELDERLY: 1.5 g (ceftolozane 1
g/tazobactam 0.5 g) q8h for 7 days.
AVAILABILITY (Rx)
b ALERT c Ceftolozane/tazobactam is a Pneumonia, Hospital-Acquired or
combination product. Ventilator-Associated
Injection, Powder for Reconstitution: 1 g IV: ADULTS, ELDERLY: 3 g (ceftolozane) q8h
ceftolozane/0.5 g tazobactam. for 7 days (longer course may be required).
Dosage in Renal Impairment
ADMINISTRATION/HANDLING CrCl 30–50 mL/min: 750 mg (500
IV mg/250 mg) q8h. CrCl 15–29 mL/
min: 375 mg (250 mg/125 mg) q8h. End-
Reconstitution • Reconstitute vial stage renal disease or on hemodialy-
with 10 mL of Sterile Water for Injection sis: 750 mg (500 mg/250 mg) loading
or 0.9% NaCl. • Shake gently until dose, then 150 mg (100 mg/50 mg)
powder is completely dissolved. • Fi- maintenance dose q8h for the remainder
nal volume of vial will equal approx. of the treatment period. Note: Admin-
11.4 mL. • Visually inspect for partic- ister after hemodialysis on hemodialysis
ulate matter or discoloration. Solution days.
should appear clear, colorless to slightly
yellow in color. • Withdraw required Dosage in Hepatic Impairment
volume from reconstituted vial and in- No dose adjustment.
ject into diluent bag containing 100 mL
0.9% NaCl or 5% dextrose injection as SIDE EFFECTS
follows: Occasional (6%–3%): Nausea, diarrhea,
Ceftolozane/ Volume to pyrexia, insomnia, headache, vomiting.
Tazobactam Withdraw from Rare (2%–1%): Constipation, anxiety,
Reconstituted Vial hypotension, rash, abdominal pain, diz-
1.5 g (1 g/0.5 g) 11.4 mL ziness, tachycardia, dyspnea, urticaria,
750 mg (500 mg/250 mg) 5.7 mL gastritis, abdominal distention, dyspep-
375 mg (250 mg/125 mg) 2.9 mL sia, flatulence.
150 mg (100 mg/50 mg) 1.2 mL
ADVERSE EFFECTS/TOXIC
Rate of administration • Infuse over REACTIONS
60 min. Clinical cure rates were lower in pts with
Storage • Refrigerate intact vi- CrCl 30–50 mL/min compared with those
als. • Reconstituted vial may be held with CrCl greater than 50mL/min, and in

underlined – top prescribed drug


cefTRIAXone 225
pts receiving metroNIDAZOLE combina- PATIENT/FAMILY TEACHING
tion therapy. Hypersensitivity reactions • It is essential to complete drug therapy
including anaphylaxis or severe skin reac- despite symptom improvement. Early dis-
tions have been reported with use of beta- continuation may result in antibacterial C
lactam antibacterial drugs. Clostridium resistance or increased risk of recurrent
difficile (C-diff)–associated diarrhea, with infection. • Report any episodes of diar-
severity ranging from mild diarrhea to fatal rhea, esp. the following mos after treat-
colitis, was reported. C-diff infection may ment completion. Frequent diarrhea, fe-
occur more than 2 mos after treatment ver, abdominal pain, blood-streaked stool
completion. May increase risk of develop- may indicate infectious diarrhea and may
ment of drug-resistant bacteria when used be contagious to others. • Report ab-
in the absence of a proven or strongly sus- dominal pain, black/tarry stools, bruising,
pected bacterial infection. Atrial fibrillation yellowing of skin or eyes; dark urine, de-
reported in 1.2% of pts. Other reported creased urine output. • Drink plenty of
adverse events such as angina pectoris, in- fluids. • Severe allergic reactions such
fections (candidiasis, oropharyngeal infec- as hives, palpitations, rash, shortness of
tion, fungal urinary tract infection), para- breath, tongue swelling may occur.
lytic ileus, venous thrombosis occur rarely.
NURSING CONSIDERATIONS cefTRIAXone
BASELINE ASSESSMENT
Obtain baseline CBC, serum BUN, cre- sef-trye-ax-own
atinine; CrCl, GFR, LFT; bacterial culture Do not confuse cefTRIAXone
and sensitivity; vital signs. Question his- with ceFAZolin, cefOXitin, or
tory of atrial fibrillation, recent C. diffi- ceftazidime.
cile infection, hepatic/renal impairment, uCLASSIFICATION
hypersensitivity reaction to beta-lactams,
cephalosporins, penicillins, carbapenem. PHARMACOTHERAPEUTIC: Third-
Assess skin for wounds; assess hydration generation cephalosporin. CLINI-
status. Question pt’s usual stool charac- CAL: Antibiotic.
teristics (color, frequency, consistency).
INTERVENTION/EVALUATION USES
Monitor CBC, BMP, renal function test Treatment of susceptible infections due to
periodically; serum magnesium, ionized gram-negative aerobic organisms, some
calcium in pts at risk for arrhythmias. For gram-positive organisms, including respira-
pts with changing renal function, monitor tory tract, GU tract, skin and skin structure,
renal function test daily and adjust dose bone and joint, intra-abdominal, pelvic in-
accordingly. Diligently monitor I&Os. Ob- flammatory disease (PID), biliary tract/uri-
serve daily pattern of bowel activity, stool nary tract infections; bacterial septicemia,
consistency (increased severity may indi- meningitis, perioperative prophylaxis, acute
cate antibiotic-associated colitis). If fre- bacterial otitis media. OFF-LABEL: Compli-
quent diarrhea occurs, obtain C. difficile cated gonococcal infections, STDs, Lyme
toxin screen and initiate isolation precau- disease, salmonellosis, shigellosis, atypical
tions until test result confirmed; manage community-acquired pneumonia.
proper fluids levels/PO intake, electrolyte
levels, protein intake. Antibacterial drugs PRECAUTIONS
that are not directed against C-diff infec- Contraindications: History of hypersensitiv-
tion may need to be discontinued. Report ity/anaphylactic reaction to cefTRIAXone,
any signs of hypersensitivity reaction. cephalosporins. Hyperbilirubinemic neo-
nates, esp. premature infants, should not
Canadian trade name Non-Crushable Drug High Alert drug
226 cefTRIAXone
be treated with cefTRIAXone (can displace mL. • May further dilute with 50–100
bilirubin from its binding to serum albu- mL 0.9% NaCl, D5W.
min, causing bilirubin encephalopathy). Rate of administration • For IV push,
C Do not administer with calcium-containing administer over 1–4 min (maximum
IV solutions, including continuous calcium- concentration: 40 mg/mL). • For inter-
containing infusion such as parenteral mittent IV infusion (piggyback), infuse
nutrition (in neonates) due to the risk of over 30 min.
precipitation of cefTRIAXone-calcium salt. Storage • Solution appears light yel-
Cautions: Hepatic impairment, history of GI low to amber. • IV infusion (piggyback)
disease (esp. ulcerative colitis, antibiotic-as- is stable for 2 days at room temperature,
sociated colitis). History of penicillin allergy. 10 days if refrigerated. • Discard if pre-
cipitate forms.
ACTION
IM
Binds to bacterial cell membranes, in-
hibits cell wall synthesis. Therapeutic • Add 0.9 mL Sterile Water for Injection,
Effect: Bactericidal. 0.9% NaCl, D5W, or lidocaine to each 250
mg to provide concentration of 250 mg/
PHARMACOKINETICS mL. • To minimize discomfort, inject deep
Widely distributed, including to CSF. Protein IM slowly. Less painful if injected into glu-
binding: 83%–96%. Primarily excreted in teus maximus than lateral aspect of thigh.
urine. Not removed by hemodialysis. Half- IV INCOMPATIBILITIES
life: IV: 4.3–4.6 hrs; IM: 5.8–8.7 hrs
(increased in renal impairment). Amphotericin B complex (Abelcet, AmBi-
some, Amphotec), famotidine (Pepcid),
LIFESPAN CONSIDERATIONS fluconazole (Diflucan), labetalol (Nor-
Pregnancy/Lactation: Readily crosses modyne), Lactated Ringer’s injection,
placenta. Distributed in breast milk. Chil- vancomycin (Vancocin).
dren: May displace bilirubin from serum IV COMPATIBILITIES
albumin. Contraindicated in hyperbilirubin-
emic neonates. Elderly: Age-related renal DiltiaZEM (Cardizem), heparin, lido-
impairment may require dosage adjustment. caine, metroNIDAZOLE (Flagyl), mor-
phine, propofol (Diprivan).
INTERACTIONS
INDICATIONS/ROUTES/DOSAGE
DRUG: Probenecid may increase excre-
Usual Dosage Range
tion. Calcium salts may increase adverse/
toxic effects. HERBAL: None significant. IM/IV: ADULTS, ELDERLY: 1–2 g q12–24h.
FOOD: None known. LAB VALUES: May
50–75
CHILDREN: Mild to moderate infection:

increase serum BUN, alkaline phosphatase, mg/kg/day in 1–2 divided doses. Maxi-
bilirubin, creatinine, LDH, ALT, AST. May mum: 2 g/day. Severe infection: 80–100 mg/
cause positive direct/indirect Coombs’ test. kg/day divided q12–24h. Maximum: 4 g/
day. NEONATES: 25–50 mg/kg/dose given
AVAILABILITY (Rx) once daily.
Injection, Powder for Reconstitution: 250 Dosage in Renal/Hepatic Impairment
mg, 500 mg, 1 g, 2 g. Intravenous Solu- Dosage modification is usually unnecessary,
tion: 1 g/50 mL, 2 g/50 mL. but hepatic/renal function test results should
be monitored in pts with renal and hepatic
ADMINISTRATION/HANDLING impairment or severe renal impairment.
IV
SIDE EFFECTS
Reconstitution • Add 2.4 mL Sterile Frequent: Discomfort with IM adminis-
Water for Injection to each 250 mg to tration, oral candidiasis (thrush), mild
provide concentration of 100 mg/ diarrhea, mild abdominal cramping,
underlined – top prescribed drug
cefuroxime 227
vaginal candidiasis. Occasional: Nausea, uCLASSIFICATION
serum sickness–like reaction (fever, joint PHARMACOTHERAPEUTIC: Second-
pain; usually occurs after second course generation cephalosporin. CLINI-
of therapy and resolves after drug is dis- CAL: Antibiotic. C
continued). Rare: Allergic reaction (rash,
pruritus, urticaria), thrombophlebitis
(pain, redness, swelling at injection site). USES
ADVERSE EFFECTS/TOXIC Treatment of susceptible infections due
REACTIONS to group B streptococci, pneumococci,
Antibiotic-associated colitis, other superin- staphylococci, H. influenzae, E. coli,
fections (abdominal cramps, severe watery Enterobacter, Klebsiella, including
diarrhea, fever) may result from altered acute/chronic bronchitis, gonorrhea, im-
bacterial balance in GI tract. Nephrotoxicity petigo, early Lyme disease, otitis media,
may occur, esp. in pts with preexisting renal pharyngitis/tonsillitis, sinusitis, skin/skin
disease. Pts with history of penicillin allergy structure, UTI, perioperative prophylaxis.
are at increased risk for developing a severe PRECAUTIONS
hypersensitivity reaction (severe pruritus,
angioedema, bronchospasm, anaphylaxis). Contraindications: History of hypersen-
sitivity/anaphylactic reaction to cefurox-
NURSING CONSIDERATIONS ime, cephalosporins. Cautions: Severe
renal impairment, history of penicillin
BASELINE ASSESSMENT
allergy. Pts with hx of colitis, GI malab-
Obtain CBC, renal function tests. Ques- sorption, seizures.
tion for history of allergies, particularly
cephalosporins, penicillins. ACTION
INTERVENTION/EVALUATION Binds to bacterial cell membranes, in-
Assess oral cavity for white patches on mu- hibits cell wall synthesis. Therapeutic
cous membranes, tongue (thrush). Moni- Effect: Bactericidal.
tor daily pattern of bowel activity, stool con- PHARMACOKINETICS
sistency. Mild GI effects may be tolerable
(increasing severity may indicate onset of Rapidly absorbed from GI tract. Protein
antibiotic-associated colitis). Monitor I&O, binding: 33%–50%. Widely distributed,
renal function tests for nephrotoxicity, CBC. including to CSF. Primarily excreted un-
Be alert for superinfection: fever, vomiting, changed in urine. Moderately removed
diarrhea, anal/genital pruritus, oral muco- by hemodialysis. Half-life: 1.3 hrs (in-
sal changes (ulceration, pain, erythema). creased in renal impairment).

PATIENT/FAMILY TEACHING LIFESPAN CONSIDERATIONS


• Discomfort may occur with IM injec- Pregnancy/Lactation: Readily crosses
tion. • Doses should be evenly placenta. Distributed in breast milk. Chil-
spaced. • Continue antibiotic therapy for dren: No age-related precautions noted.
full length of treatment. Elderly: Age-related renal impairment
may require dosage adjustment.
cefuroxime INTERACTIONS
sef-ue-rox-eem DRUG: Probenecid may increase con-
(Ceftin) centration. Antacids, H2-receptor
Do not confuse Ceftin with Cefzil antagonists (e.g., cimetidine, fa-
or Cipro, cefuroxime with cefo- motidine), proton pump inhibitors
taxime, cefprozil, or deferoxam- (e.g., pantoprazole) may decrease ab-
ine, or Zinacef with Zithromax. sorption. May decrease therapeutic effect
Canadian trade name Non-Crushable Drug High Alert drug
228 cefuroxime
of BCG (intravesical). HERBAL: None IV COMPATIBILITIES
significant. FOOD: None known. LAB DiltiaZEM (Cardizem), HYDROmorphone
VALUES: May increase serum BUN, cre- (Dilaudid), morphine, propofol (Diprivan).
C atinine, alkaline phosphatase, bilirubin,
LDH, ALT, AST. May cause positive direct/ INDICATIONS/ROUTES/DOSAGE
indirect Coombs’ test. Usual Dosage
IV, IM: ADULTS, ELDERLY, CHILDREN 12 YRS
AVAILABILITY (Rx) AND OLDER: 750 mg–1.5 g q8h up to 1.5 g
Injection, Powder for Reconstitution: 750 q6h for severe infections. CHILDREN: 3 MOS
mg, 1.5 g. Oral Suspension: 125 mg/5 TO YOUNGER THAN 12 YRS: Mild to moderate
mL, 250 mg/5 mL. Tablets: 250 mg, 500 infection: 75–100 mg/kg/day divided q8h.
mg. Maximum: 1,500 mg/dose. Severe infec-
tion: 100–200 mg/kg/day divided into 3–4
ADMINISTRATION/HANDLING doses. Maximum: 1,500 mg/dose. NEO-
IV NATES: 50 mg/kg/dose q8–12h.
PO: ADULTS, ELDERLY, CHILDREN 12 YRS
Reconstitution • Reconstitute 750 AND OLDER: 250–500 mg twice a day.
mg in 8 mL (1.5 g in 14 mL) Sterile Wa- CHILDREN 3 MOS TO YOUNGER THAN 12
ter for Injection to provide a concentra- YRS: 20–30 mg/kg/day in 2 divided doses.
tion of 100 mg/mL. • For intermittent Maximum: 1 g/day (500 mg/dose).
IV infusion (piggyback), further dilute
with 50–100 mL 0.9% NaCl or D5W. Dosage in Renal Impairment
Rate of administration • For IV Adult dosage frequency is modified based
push, administer over 3–5 min. • For on creatinine clearance and severity of
intermittent IV infusion (piggyback), in- infection.
fuse over 15–30 min. Creatinine Clearance Dosage
Storage • Solution appears light yel- IV
low to amber (may darken, but color Greater than 20 mL/min q8h
change does not indicate loss of po- 10–20 mL/min q12h
tency). • IV infusion (piggyback) is Less than 10 mL/min q24h
stable for 24 hrs at room temperature, 7 Peritoneal dialysis Dose q24h
Continuous renal re- 1 g q12h
days if refrigerated. • Discard if pre-
placement therapy
cipitate forms. PO
Greater than 30 mL/min No adjustment
IM 10–29 mL/min q24h
• To minimize discomfort, inject deep Less than 10 mL/min q48h
IM slowly in large muscle mass.
Dosage in Hepatic Impairment
PO No dose adjustment.
• Give tablets without regard to food
(give 400-mg dose with food). • If GI SIDE EFFECTS
upset occurs, give with food, milk. • Frequent: Discomfort with IM adminis-
Avoid crushing tablets due to bitter tration, oral candidiasis (thrush), mild
taste. • Suspension must be given diarrhea, mild abdominal cramping,
with food. • Suspension stable at vaginal candidiasis. Occasional: Nausea,
room temperature or refrigerated for serum sickness–like reaction (fever, joint
10 days. pain; usually occurs after second course
of therapy and resolves after drug is dis-
IV INCOMPATIBILITIES continued). Rare: Allergic reaction (rash,
Fluconazole (Diflucan), midazolam pruritus, urticaria), thrombophlebitis
(Versed), vancomycin (Vancocin). (pain, redness, swelling at injection site).

underlined – top prescribed drug


celecoxib 229

ADVERSE EFFECTS/TOXIC uCLASSIFICATION


REACTIONS PHARMACOTHERAPEUTIC: NSAID,
Antibiotic-associated colitis, other super- COX-2 selective. CLINICAL: Anti-
infections (abdominal cramps, severe inflammatory. C
watery diarrhea, fever) may result from
altered bacterial balance in GI tract.
Nephrotoxicity may occur, esp. in pts with USES
preexisting renal disease. Pts with history Relief of signs/symptoms of osteoarthri-
of penicillin allergy are at increased risk tis, rheumatoid arthritis (RA) in adults.
for developing a severe hypersensitivity Treatment of acute pain, primary dys-
reaction (severe pruritus, angioedema, menorrhea. Relief of signs/symptoms
bronchospasm anaphylaxis). associated with ankylosing spondylitis.
Treatment of juvenile rheumatoid ar-
NURSING CONSIDERATIONS thritis (JRA) in pts 2 yrs and older and
BASELINE ASSESSMENT
weighing 10 kg or more.
Obtain CBC, renal function tests. Ques- PRECAUTIONS
tion for history of allergies, particularly b ALERT c May increase cardiovascu-
cephalosporins, penicillins. lar risk when high doses are given to
INTERVENTION/EVALUATION prevent colon cancer.
Contraindications: Hypersensitivity to
Assess oral cavity for white patches on mu-
cous membranes, tongue (thrush). Moni- celecoxib, sulfonamides, aspirin, other
tor daily pattern of bowel activity, stool con- NSAIDs. Active GI bleeding. Pts expe-
sistency. Mild GI effects may be tolerable riencing asthma, urticaria, or allergic
(increasing severity may indicate onset of reactions to aspirin, other NSAIDs.
antibiotic-associated colitis). Monitor I&O, Treatment of perioperative pain in coro-
renal function tests for nephrotoxicity. Be nary artery bypass graft (CABG) surgery.
Cautions: History of GI disease (bleed-
alert for superinfection: fever, vomiting, di-
arrhea, anal/genital pruritus, oral mucosal ing/ulcers); concurrent use with aspi-
changes (ulceration, pain, erythema). rin, anticoagulants, smoking; alcohol,
elderly, debilitated pts, hypertension,
PATIENT/FAMILY TEACHING asthma, renal/hepatic impairment. Pts
• Discomfort may occur with IM injec- with edema, cerebrovascular disease,
tion. • Doses should be evenly ischemic heart disease, HF, known or
spaced. • Continue antibiotic therapy suspected deficiency of cytochrome
for full length of treatment. • May cause P450 isoenzyme 2C9. Pediatric pts with
GI upset (may take with food, milk). systemic-onset juvenile idiopathic ar-
thritis.
ACTION
celecoxib Inhibits cyclooxygenase-2, the enzyme
sel-e-kox-ib responsible for prostaglandin synthesis.
(CeleBREX) Therapeutic Effect: Reduces inflam-
mation, relieves pain.
j BLACK BOX ALERT jIncreased
risk of serious cardiovascular throm-
botic events, including MI, CVA. PHARMACOKINETICS
Increased risk of severe GI reac- Rapidly absorbed from GI tract. Widely
tions, including ulceration, bleeding, distributed. Protein binding: 97%. Me-
perforation of stomach, intestines. tabolized in liver. Primarily eliminated in
Do not confuse CeleBREX with feces. Half-life: 11.2 hrs.
CeleXA, Cerebyx, or Clarinex.

Canadian trade name Non-Crushable Drug High Alert drug


230 celecoxib

LIFESPAN CONSIDERATIONS Acute Pain, Primary Dysmenorrhea


PO: ADULTS, ELDERLY: Initially, 400
mg
Pregnancy/Lactation: Unknown if
with additional 200 mg on day 1, if
drug crosses placenta or is distributed in
C needed. Maintenance: 200 mg twice
breast milk. Avoid use during third trimes-
daily as needed.
ter (may adversely affect fetal cardiovascu-
lar system: premature closure of ductus Ankylosing Spondylitis
arteriosus). Children: Safety and efficacy PO: ADULTS, ELDERLY: 200 mg/day as a
not established. Elderly: No age-related single dose or in 2 divided doses. May in-
precautions noted. crease to 400 mg/day if no effect is seen
after 6 wks.
INTERACTIONS
DRUG: May increase concentration of Dosage in Renal Impairment
lithium, methotrexate. Aspirin may Not recommended in severe renal im-
increase adverse effects. May increase pairment.
nephrotoxic effects of cycloSPORINE,
tenofovir. HERBAL: Herbals with an- Dosage in Hepatic Impairment
ticoagulant/antiplatelet properties Decrease dose by 50% in pts with mod-
(e.g., garlic, ginger, ginkgo biloba) erate hepatic impairment. Not recom-
may increase adverse effects. FOOD: None mended in severe hepatic impairment.
known. LAB VALUES: May increase serum
ALT, AST, alkaline phosphatase, creatinine, SIDE EFFECTS
BUN. May decrease serum phosphate. Frequent (16%–5%): Diarrhea, dyspepsia,
headache, upper respiratory tract infec-
AVAILABILITY (Rx) tion. Occasional (less than 5%): Abdomi-
Capsules: 50 mg, 100 mg, 200 mg, nal pain, flatulence, nausea, back pain,
400 mg. peripheral edema, dizziness, insomnia,
rash.
ADMINISTRATION/HANDLING
ADVERSE EFFECTS/TOXIC
PO REACTIONS
• May give without regard to food.
• Capsules may be swallowed whole or Increased risk of cardiovascular events
opened and mixed with applesauce. (MI, CVA), serious, potentially life-­
threatening GI bleeding.
INDICATIONS/ROUTES/DOSAGE
NURSING CONSIDERATIONS
Note: Consider reduced initial dose of
50% in poor CYP2C9 metabolizers. BASELINE ASSESSMENT
Assess onset, type, location, duration of
Osteoarthritis pain/inflammation. Inspect appearance
PO: ADULTS, ELDERLY: 200 mg/day as a of affected joints for immobility, defor-
single dose or 100 mg twice daily. mity, skin condition. Assess for allergy
Rheumatoid Arthritis (RA)
to sulfa, aspirin, or NSAIDs (contraindi-
PO: ADULTS, ELDERLY: 100–200 mg cated).
twice daily. INTERVENTION/EVALUATION

Juvenile Rheumatoid Arthritis (JRA)


Assess for therapeutic response: pain
PO: CHILDREN 2 YRS AND OLDER, WEIGH-
relief; decreased stiffness, swelling;
ING MORE THAN 25 KG: 100 mg twice increased joint mobility; reduced joint
daily. WEIGHING 10–25 KG: 50 mg twice tenderness; improved grip strength.
daily. Observe for bleeding, bruising, weight
gain.

underlined – top prescribed drug


cephalexin 231
PATIENT/FAMILY TEACHING PHARMACOKINETICS
• If GI upset occurs, take with Rapidly absorbed from GI tract (delayed
food. • Avoid aspirin, alcohol (in- in young children). Protein binding: 10%–
creases risk of GI bleeding). • Immedi- 15%. Widely distributed. Primarily excreted C
ately report chest pain, jaw pain, sweat- unchanged in urine. Moderately removed
ing, confusion, difficulty speaking, by hemodialysis. Half-life: 0.9–1.2 hrs
one-sided weakness (may indicate heart (increased in renal impairment).
attack or stroke).
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Readily crosses
placenta. Distributed in breast milk. Chil-
cephalexin dren: No age-related precautions noted.
Elderly: Age-related renal impairment
sef-a-lex-in may require dosage adjustment.
(Keflex)
Do not confuse cephalexin with
INTERACTIONS
cefaclor, ceFAZolin, or cipro- DRUG: Probenecid may increase con-
floxacin. centration. HERBAL: None significant.
FOOD: None known. LAB VALUES: May
uCLASSIFICATION increase serum BUN, creatinine, alkaline
PHARMACOTHERAPEUTIC: First- phosphatase, bilirubin, LDH, ALT, AST. May
generation cephalosporin. CLINI- cause positive direct/indirect Coombs’ test.
CAL: Antibiotic.
AVAILABILITY (Rx)
Capsules: 250 mg, 500 mg, 750 mg.
USES Powder for Oral Suspension: 125 mg/5
mL, 250 mg/5 mL. Tablets: 250 mg,
Treatment of susceptible infections due 500 mg.
to staphylococci, group A streptococcus,
K. pneumoniae, E. coli, P. mirabilis, H. ADMINISTRATION/HANDLING
influenzae, M. catarrhalis, including re- PO
spiratory tract, genitourinary tract, skin, • After reconstitution, oral suspension
soft tissue, bone infections; otitis media; is stable for 14 days if refriger-
follow-up to parenteral therapy. OFF- ated. • Shake oral suspension well be-
LABEL: Suppression of prosthetic joint
fore using. • Give without regard to
infection. food. If GI upset occurs, give with food,
PRECAUTIONS milk.
Contraindications: History of hyper- INDICATIONS/ROUTES/DOSAGE
sensitivity/anaphylactic reaction to Usual Dosage Range
cephalexin, cephalosporins. Cau- PO: ADULTS, ELDERLY: 250–1,000 mg
tions: Renal impairment, history of
q6h or 500 mg q12h. Maximum: 4 g/
GI disease (esp. ulcerative colitis, day. CHILDREN 1 YR AND OLDER: 25–100
antibiotic-associated colitis), history mg/kg/day in 3–4 divided doses. Maxi-
of penicillin allergy. mum: 4 g/day.
ACTION Dosage in Renal Impairment
Binds to bacterial cell membranes, in- After usual initial dose, dosing frequency
hibits cell wall synthesis. Therapeutic is modified based on creatinine clear-
Effect: Bactericidal. ance and severity of infection.

Canadian trade name Non-Crushable Drug High Alert drug


232 ceritinib
Creatinine for nephrotoxicity. Be alert for superinfec-
Clearance Dosage tion: fever, vomiting, diarrhea, anal/genital
60 mL/min or No adjustment pruritus, oral mucosal changes (ulceration,
C greater pain, erythema). With prolonged therapy,
30–59 mL/min Maximum: 1,000 mg/day monitor renal/hepatic function tests.
15–29 mL/min 250 mg q8-12h
5–14 mL/min 250 mg q24h PATIENT/FAMILY TEACHING
1–4 mL/min 250 mg q48-60h • Doses should be evenly spaced.
Hemodialysis 250–500 mg q12–24h
(administer after dialy-
• Continue therapy for full length of
sis session) treatment. • May cause GI upset (may
take with food, milk). • Refrigerate
Dosage in Hepatic Impairment oral suspension. • Report persistent
No dose adjustment. diarrhea.
SIDE EFFECTS
Frequent: Oral candidiasis, mild diar- ceritinib
rhea, mild abdominal cramping, vaginal
candidiasis. Occasional: Nausea, serum se-ri-ti-nib
sickness–like reaction (fever, joint pain; (Zykadia)
usually occurs after second course of Do not confuse ceritinib with
therapy and resolves after drug is discon- crizotinib, gefitinib, imatinib,
tinued). Rare: Allergic reaction (rash, or lapatinib.
pruritus, urticaria).
uCLASSIFICATION
ADVERSE EFFECTS/TOXIC PHARMACOTHERAPEUTIC: Anaplas-
REACTIONS tic lymphoma kinase inhibitor. CLINI-
Antibiotic-associated colitis, other super- CAL: Antineoplastic.
infections (abdominal cramps, severe
watery diarrhea, fever) may result from
altered bacterial balance in GI tract. USES
Nephrotoxicity may occur, esp. in pts with Treatment of pts with anaplastic lym-
preexisting renal disease. Pts with history phoma kinase (ALK)–positive metastatic
of penicillin allergy are at increased risk non–small-cell lung cancer (NSCLC).
for developing a severe hypersensitivity
reaction (severe pruritus, angioedema, PRECAUTIONS
bronchospasm, anaphylaxis). Contraindications: Hypersensitivity to
NURSING CONSIDERATIONS ceritinib. Cautions: Bradyarrhythmias/
ventricular arrhythmias, diabetes, de-
BASELINE ASSESSMENT hydration, electrolyte imbalance (e.g.,
Obtain CBC, renal function tests. Ques- hypomagnesemia, hypokalemia), hepatic
tion for history of allergies, particularly impairment, HF, ocular disease, pulmo-
cephalosporins, penicillins. nary disease. Medications that prolong
QT interval. Not recommended in pts with
INTERVENTION/EVALUATION congenital long QT syndrome. Avoid use
Assess oral cavity for white patches on of medications that cause bradycardia.
mucous membranes, tongue (thrush).
Monitor daily pattern of bowel activity, ACTION
stool consistency. Mild GI effects may Potent inhibitor of ALK involved in the
be tolerable (increasing severity may pathogenesis of NSCLC. ALK gene ab-
indicate onset of antibiotic-associated normalities may result in expression of
colitis). Monitor I&O, renal function tests oncogenic fusion proteins, resulting in
underlined – top prescribed drug
ceritinib 233
increased cell proliferation/survival in tu- is missed, take dose unless next dose due
mor cells. Therapeutic Effect: Reduces within 12 hrs. If vomiting occurs, do not
proliferation of tumor cells expressing administer an additional dose.
the genetic abnormality. C
INDICATIONS/ROUTES/DOSAGE
PHARMACOKINETICS Non–Small-Cell Lung Cancer
Well absorbed after PO administration. PO: ADULTS/ELDERLY: 450 mg once daily
Metabolized in liver. Peak plasma con- until disease progression or unaccept-
centration: 4–6 hrs. Protein binding: able toxicity.
97%. Eliminated in feces (92%), urine
(1.3%). Half-life: 41 hrs. Dosage in Renal Impairment
Mild to moderate impairment: CrCl
LIFESPAN CONSIDERATIONS 30–90 mL/min: No dose adjustment.
Pregnancy/Lactation: Avoid preg- Severe impairment: Not specified; use
nancy; may cause fetal harm. Do not initiate caution.
therapy until pregnancy status confirmed.
Contraception recommended during treat- Dosage in Hepatic Impairment
ment and for at least 2 wks after discon- Mild to moderate impairment: No
tinuation. Unknown if distributed in breast dose adjustment. Severe impairment:
milk. Must either discontinue drug or dis- Decrease dose by 1/3 (round to nearest
continue breastfeeding. Children: Safety 150 mg).
and efficacy not established. Elderly: No
Dose Modification
age-related precautions noted.
Cardiac
INTERACTIONS QTc interval greater than 500 msec
on at least 2 separate ECGs: Withhold
DRUG: Strong CYP3A inhibitors
(e.g., ketoconazole, ritonavir) may until QTc interval is less than 481 msec, or
increase concentration/effect; avoid use. recovery to baseline (if baseline QTc inter-
Strong CYP3A inducers (e.g., car- val is greater than or equal to 481 msec),
BAMazepine, phenytoin, rifAMPin) then resume with a 150-mg dose reduction.
QTc prolongation in combination
may decrease concentration/effect; avoid
with torsades de pointes or polymor-
use. Amiodarone, dronedarone may
phic ventricular tachycardia or serious
increase risk of bradycardia. May increase
arrhythmia: Permanently discontinue.
concentration/effects of aprepitant, bo-
Symptomatic, non–life-threatening
sutinib, budesonide, cobimetinib,
bradycardia: Withhold until recovery
colchicine, eletriptan, ivabradine.
HERBAL: St. John’s wort may decrease
to asymptomatic bradycardia or heart
effectiveness. FOOD: All food may in- rate of 60 beats/min or greater. Evaluate
crease absorption/effect. Grapefruit concomitant medications known to cause
products may increase concentration/ef- bradycardia and adjust dose as tolerated
fect; avoid use. LAB VALUES: May decrease (reduction not specified).
Clinically significant, life-threatening
Hgb, phosphate. May increase serum ALT,
bradycardia requiring intervention
AST, bilirubin, creatinine, glucose, lipase.
or life-threatening bradycardia in
AVAILABILITY (Rx) pts taking concomitant medications
known to cause bradycardia or hy-
Capsules: 150 mg. potension: Withhold until recovery to
ADMINISTRATION/HANDLING asymptomatic bradycardia or heart rate
of 60 beats/min or greater. If concomitant
PO medication can be adjusted or discon-
• Give with food. • Administer whole; tinued, then resume with a 150-mg dose
do not break, cut, or open. • If a dose reduction.
Canadian trade name Non-Crushable Drug High Alert drug
234 ceritinib
Life-threatening bradycardia in pts thenia. Occasional (34%–9%): Decreased
who are not taking concomitant medi- appetite, constipation, paresthesia,
cations known to cause bradycardia or muscular weakness, gait disturbance,
C hypotension: Permanently discontinue. peripheral motor/sensory neuropathy,
Concomitant use of strong CYP3A in- hypotonia, polyneuropathy, dyspepsia,
hibitors: If concomitant use unavoidable, gastric reflux disease, dysphagia, rash,
reduce ceritinib dose by one third, rounded maculopapular rash, acneiform derma-
to the nearest 150-mg dose strength. After titis, vision impairment, blurred vision,
discontinuation of a strong CYP3A inhibitor, photopsia, presbyopia, reduced visual
resume ceritinib dose that was taken prior acuity.
to initiating strong CYP3A inhibitor.
Endocrine
ADVERSE EFFECTS/TOXIC
Persistent hyperglycemia greater
REACTIONS
than 250 mL/dL despite optimal an- Approximately 60% of pts required at least
tihyperglycemic therapy: Withhold one dose reduction. Median time to first
until hyperglycemia is adequately con- dose reduction was approximately 7 wks.
trolled, then resume with a 150-mg dose Decreased Hgb levels reported in 84% of
reduction. If adequate control cannot be pts. Severe or persistent GI toxicity includ-
achieved with optimal medical manage- ing nausea, vomiting, diarrhea occurred in
ment, then permanently discontinue. 96% of pts; severe cases reported in 14%
of pts. Drug-induced hepatotoxicity with
Gastrointestinal elevation of serum ALT 5 times ULN oc-
Severe or intolerable diarrhea, curred in 27% of pts. Bradycardia, severe
nausea, vomiting despite optimal interstitial lung disease (ILD), QT interval
antiemetic or antidiarrheal ther- prolongation, ILD reported in 3% of pts.
apy: Withhold until improved, then re- Grade 3–4 hyperglycemia reported in 13%
sume with a 150-mg dose reduction. of pts; diabetics have a sixfold increase in
Hepatic (During Treatment) risk; pts receiving corticosteroids have
ALT, AST greater than 5 times upper twofold increase in risk. Fatal adverse re-
limit of normal (ULN) with total bili- actions including pneumonia, respiratory
rubin elevation less than or equal to failure, ILD/pneumonitis, pneumothorax,
2 times ULN: Withhold until recovery to gastric hemorrhage, general physical
baseline or less than or equal to 2 times ULN, health deterioration, tuberculosis, cardiac
then resume with a 150-mg dose reduction. tamponade, sepsis occurred in 5% of pts.
ALT, AST greater than 3 times ULN
with total bilirubin elevation greater NURSING CONSIDERATIONS
than or equal to 2 times ULN in the BASELINE ASSESSMENT
absence of cholestasis or hemoly-
Obtain baseline CBC, BMP, LFT; serum
sis: Permanently discontinue.
ionized calcium, magnesium, phosphate;
Pulmonary capillary blood glucose, O2 saturation,
Any grade treatment related to in- urine pregnancy, vital signs. Obtain base-
terstitial lung disease/pneumoni- line ECG in pts with history of arrhythmias,
tis: Permanently discontinue. HF, electrolyte imbalance, or concurrent
use of medications known to prolong QTc
Intolerability/Toxicity interval. Question possibility of pregnancy
If unable to tolerate 300-mg dose: or plans of breastfeeding. Assess hydra-
Permanently discontinue. tion status. Screen for history/co-mor-
SIDE EFFECTS bidities. Receive full medication history
Frequent (86%–52%): Diarrhea, nausea, including herbal products; esp. CYP3A
vomiting, abdominal pain, fatigue, as- inhibitors or inducers, medications that

underlined – top prescribed drug


certolizumab pegol 235
prolong QT interval. Assess visual acuity.
Verify ALK-positive NSCLC test prior to certolizumab pegol
initiation.
ser-toe-liz-ue-mab C
INTERVENTION/EVALUATION (Cimzia)
Monitor CBC routinely; LFT monthly (or j BLACK BOX ALERT jSerious,
more frequently in pts with elevated he- sometimes fatal cases of tubercu-
patic enzymes). Obtain BMP, serum ion- losis, invasive fungal infections, or
ized calcium, magnesium if arrhythmia other opportunistic infections, in-
cluding viral and bacterial infection,
or dehydration occurs. Monitor vital have been reported. Lymphoma
signs (esp. heart rate). Obtain ECG for reported in children/adolescents
bradycardia, chest pain, dyspnea; chest receiving other TNF-blocking
X-ray if ILD, pneumonitis, pneumothorax medications.
suspected. Worsening cough, fever, or
uCLASSIFICATION
shortness of breath may indicate pneu-
monitis. Monitor for hepatic dysfunction, PHARMACOTHERAPEUTIC: Anti-
hyperglycemia, sepsis, vision changes. rheumatic, disease modifying. GI
Assess hydration status. Encourage PO agent. Tumor necrosis factor (TNF)
intake. Offer antidiarrheal medication blocker. CLINICAL: Anti-inflammato-
for loose stool, antiemetic for nausea, ry agent.
vomiting.
PATIENT/FAMILY TEACHING USES
• Blood levels, ECGs will be monitored Treatment of moderate to severe ac-
routinely. • Most pts experience diar- tive rheumatoid arthritis, moderate to
rhea, nausea, vomiting, which may lead severe active Crohn’s disease, active
to dehydration; drink plenty of flu- ankylosing spondylitis, active psoriatic
ids. • Report history of heart problems, arthritis, moderate to severe plaque
including extremity swelling, HF, con- psoriasis, axial spondyloarthritis, non-
genital long QT syndrome, palpitations, radiographic.
syncope. Therapy may decrease your
heart rate; report dizziness, chest pain, PRECAUTIONS
palpitations, or fainting. • Worsening Contraindications: Hypersensitivity to
cough, fever, or shortness of breath may certolizumab. Cautions: Chronic, latent,
indicate severe lung inflamma- or localized infection; preexisting or re-
tion. • Avoid pregnancy; contraception cent-onset CNS demyelinating disorders,
recommended during treatment and up moderate to severe HF, underlying hema-
to 2 wks after final dose. Do not breast- tologic disorders, elderly. Pts who have
feed. • Blurry vision, confusion, fre- resided in regions where TB is endemic,
quent urination, increased thirst, fruity pts who are hepatitis B virus carriers. Use
breath may indicate high blood sugar of live vaccines.
levels. • Report any yellowing of skin
or eyes, upper abdominal pain, bruising, ACTION
black/tarry stools, dark urine. • Imme- Binds to and neutralizes human TNF-alpha
diately report any newly prescribed med- activity. Elevated levels of TNF-alpha play a
ications. • Take on empty stomach role in inflammation (Crohn’s disease)
only; do not eat 2 hrs before or 2 hrs af- and joint destruction (RA). Therapeutic
ter any dose. • Avoid alcohol. Do not Effect: Reduces signs and symptoms of
consume grapefruit products. Crohn’s disease and joint destruction as-
sociated with rheumatoid arthritis.

Canadian trade name Non-Crushable Drug High Alert drug


236 certolizumab pegol

PHARMACOKINETICS INDICATIONS/ROUTES/DOSAGE
Higher clearance with increasing body Note: Each 400-mg dose is given as two
weight. Peak plasma concentrations: injections of 200 mg each.
C 54–171 hrs. Half-life: 14 days.
Crohn’s Disease
LIFESPAN CONSIDERATIONS SQ: Initially, 400mg (given as two sub-
Pregnancy/Lactation: Unknown if dis- cutaneous injections of 200 mg) and at
tributed in breast milk. Children: Safety weeks 2 and 4. Maintenance: In pts
and efficacy not established. Elderly: Use who obtain a therapeutic response, 400
cautiously due to higher rate of infection. mg q4wks.
INTERACTIONS Rheumatoid Arthritis, Ankylosing
DRUG: May increase adverse effects of Spondylitis, Psoriatic Arthritis
abatacept, anakinra, canakinumab, SQ: ADULTS, ELDERLY: Initially, 400 mg
natalizumab, vaccines (live), ve- and at weeks 2 and 4. Maintenance: 200
dolizumab. May decrease therapeutic mg q2wks or 400 mg q4wks.
effects of BCG (intravesical), vaccines
Plaque Psoriasis
(live). HERBAL: Echinacea may de-
SQ: ADULTS, ELDERLY: 400 mg every other
crease effect. FOOD: None known. LAB
VALUES: May increase serum alkaline
week. PTS WEIGHING 90 KG OR LESS: 400
phosphatase, ALT, AST, bilirubin; aPTT. mg at wks 0, 2, and 4, Then, 200 mg q
other wk may be used.
AVAILABILITY (Rx)
Axial Spondyloarthritis, Nonradiographic
Injection, Powder for Reconstitution: 200 SQ: ADULTS, ELDERLY: Initially, 400 mg,
mg. Injection, Solution: 200 mg/mL in a repeat dose 2 and 4 wks after initial dose.
single-use prefilled syringe. Maintenance: 200 mg q2wks or 400 mg
ADMINISTRATION/HANDLING q4wks.
SQ Dosage Modification
Reconstitution • Bring to room tem- Discontinue for hypersensitivity reaction,
perature before reconstitution. • Recon- lupus-like syndrome, serious infection,
stitute with 1 mL Sterile Water for Injec- sepsis, hepatitis B virus reactivation.
tion. • Gently swirl without shaking, using
syringe with 20-gauge needle. • Leave Dosage in Renal/Hepatic Impairment
undisturbed to fully reconstitute (may take No dose adjustment.
as long as 30 min). • Using a new
20-gauge needle, withdraw reconstituted SIDE EFFECTS
solution into syringe for final concentration Occasional (6%): Arthralgia. Rare (less
of 1 mL (200 mg). Use separate syringes for than 1%): Abdominal pain, diarrhea.
multiple vials. • Switch each 20-gauge
needle to a 23-gauge needle and inject full ADVERSE EFFECTS/TOXIC
contents of each syringe subcutaneously REACTIONS
into separate sites on the abdomen or thigh. Upper respiratory tract infection occurs
Storage • Store vial in refrigera- in 20% of pts. UTI occurs in 7% of pts.
tor. • Once powder reconstituted, solu- Serious infections such as pneumonia,
tion should appear clear to opalescent, pyelonephritis occur in 3% of pts. Hy-
colorless to pale yellow. • Discard if persensitivity reaction (rash, urticaria,
solution is discolored or contains pre- hypotension, dyspnea) occurs rarely.
cipitate. • Reconstituted solution is May increase risk of malignancies (e.g.,
stable for up to 2 hrs at room tempera- lymphoma).
ture or 24 hrs if refrigerated.
underlined – top prescribed drug
cetirizine 237

NURSING CONSIDERATIONS ACTION


Competes with histamine for H1-receptor
BASELINE ASSESSMENT sites on effector cells in GI tract, blood
Obtain baseline CBC, urinalysis, C-re- vessels, respiratory tract. Therapeu- C
active protein. Do not initiate treatment tic Effect: Prevents allergic response,
in pts with active infections, including produces mild bronchodilation, blocks
chronic or localized infection. TB test histamine-induced bronchitis.
should be obtained before initiation.
PHARMACOKINETICS
INTERVENTION/EVALUATION
Route Onset Peak Duration
Monitor pts for infection during and after
PO Less than 4–8 hrs Less than
treatment. If pt develops an infection, treat- 1 hr 24 hrs
ment should be discontinued. Monitor lab
results, especially WBC count, urinalysis, Well absorbed from GI tract. Protein
C-reactive protein for evidence of infection. binding: 93%. Undergoes low first-pass
PATIENT/FAMILY TEACHING
metabolism; not extensively metabo-
lized. Primarily excreted in urine. Half-
• Report cough, fever, flu-like symp- life: 6.5–10 hrs.
toms. • Do not receive live virus vac-
cine during treatment or within 3 mos LIFESPAN CONSIDERATIONS
after last dose. Pregnancy/Lactation: Not recom-
mended during first trimester of pregnancy.
Distributed in breast milk. Breastfeeding
cetirizine not recommended. Children: Less likely
to cause anticholinergic effects. Elder-
se-teer-i-zeen ly: More sensitive to anticholinergic effects
(Apo-Cetirizine , Reactine , (e.g., dry mouth, urinary retention). Dizzi-
ZyrTEC ALLERGY) ness, sedation, confusion may occur.
Do not confuse cetirizine with
levocetirizine, or ZyrTEC with INTERACTIONS
Xanax, Zantac, Zocor, or ZyPREXA. DRUG: Alcohol, other CNS depressants
may increase CNS depression. Anticho-
FIXED-COMBINATION(S) linergics (e.g., aclidinium, ipratro-
ZyrTEC D 12 Hour Tablets: cetiri- pium, umeclidinium) may increase
zine/pseudoephedrine: 5 mg/120 mg. anticholinergic effect. HERBAL: Herbs
with sedative properties (e.g., chamo-
uCLASSIFICATION
mile, kava kava, valerian) may increase
PHARMACOTHERAPEUTIC: Hista- CNS depression. FOOD: None known. LAB
mine H1 antagonist (second genera- VALUES: May suppress wheal and flare re-
tion). CLINICAL: Antihistamine. actions to antigen skin testing unless drug is
discontinued 4 days before testing.
USES
AVAILABILITY (Rx)
Relief of symptoms (sneezing, rhinorrhea,
postnasal discharge, nasal pruritus, ocu- Capsules: 10 mg. Oral Solution: 5
lar pruritus, tearing) of upper respiratory mg/5 mL. Tablets: 5 mg, 10 mg. Tablets
allergies; relieves itching due to urticaria. (Chewable): 5 mg, 10 mg. Tablets (Dis-
persible): 10 mg.
PRECAUTIONS
Contraindications: Hypersensitivity to ce- ADMINISTRATION/HANDLING
tirizine, hydrOXYzine. Cautions: Elderly, PO
hepatic/renal impairment. • Give without regard to food.
Canadian trade name Non-Crushable Drug High Alert drug
238 cetuximab

INDICATIONS/ROUTES/DOSAGE PATIENT/FAMILY TEACHING


b ALERT c May cause drowsiness at • Avoid tasks that require alertness, mo-
dosage greater than 10 mg/day. tor skills until response to drug is estab-
C lished. • Avoid alcohol.
Upper Respiratory Allergies, Urticaria
PO: ADULTS, CHILDREN OLDER THAN 5
YRS: Initially, 5–10 mg/day as single cetuximab
dose. Maximum: 10 mg/day. EL-
DERLY: 5 mg once daily. Maximum: 5 se-tux-i-mab
mg/day. CHILDREN 2–5 YRS: 2.5 mg/day. (Erbitux)
May increase up to 5 mg/day as a single j BLACK BOX ALERT j Severe
dose or in 2 divided doses. CHILDREN infusion reactions (bronchospasm,
12–23 MOS: Initially, 2.5 mg/day. May
stridor, urticaria, hypotension, cardi-
ac arrest) have occurred, especially
increase up to 5 mg/day in 2 divided with first infusion in pts with head
doses. CHILDREN 6–11 MOS: 2.5 mg and neck cancer. Cardiopulmonary
once daily. arrest reported in pts receiving radia-
tion in combination with cetuximab.
Dosage in Renal Impairment Do not confuse cetuximab with
ADULT: GFR 50 mL/min or less: 5 mg bevacizumab.
once daily. CHILDREN: GFR 10–29 mL/
min: reduce dose by 50 %. GFR <10 mL/ uCLASSIFICATION
min: Not recommended. PHARMACOTHERAPEUTIC: Epider-
mal growth factor receptor (EGFR)
Dosage in Hepatic Impairment
inhibitor, monoclonal antibody. CLINI-
No dose adjustment. CAL: Antineoplastic.
SIDE EFFECTS
Occasional (10%–2%): Pharyngitis, dry USES
mucous membranes, nausea, vomiting, Colorectal cancer, metastatic: Treat-
abdominal pain, headache, dizziness, fa- ment of KRAS wild type, EGFR-expressing,
tigue, thickening of mucus, drowsiness, metastatic colorectal cancer as first-line
photosensitivity, urinary retention. treatment (in combination with FOLFIRI
[irinotecan, fluorouracil, and leucovo-
ADVERSE EFFECTS/TOXIC rin]); in combination with irinotecan in
REACTIONS pts refractory or intolerant to irinotecan-
Children may experience paradoxical re- based chemotherapy; or as a single agent
action (restlessness, insomnia, euphoria, in pts who failed irinotecan- and oxali-
nervousness, tremor). Dizziness, seda- platin-based chemotherapy or who are
tion, confusion more likely to occur in intolerant to irinotecan. Head and neck
elderly. cancer, squamous cell: Treatment of
advanced squamous cell cancer of head/
NURSING CONSIDERATIONS neck (with radiation). Treatment of recur-
BASELINE ASSESSMENT rent or metastasized squamous cell carci-
Assess lung sounds. Assess severity of rhi- noma of head/neck progressing after plat-
nitis, urticaria, other symptoms. inum-based therapy. First-line treatment
of squamous cell carcinoma of head and
INTERVENTION/EVALUATION neck in combination with platinum-based
For upper respiratory allergies, increase therapy with 5-FU. OFF-LABEL: EGFR-
fluids to maintain thin secretions and expressing advanced non–small-cell lung
offset thirst. Monitor symptoms for thera- cancer (NSCLC). Treatment of unresect-
peutic response. able squamous cell skin cancer.

underlined – top prescribed drug


cetuximab 239

PRECAUTIONS infused over 60 min. • Maximum infu-


Contraindications: Hypersensitivity to ce- sion rate should not exceed 5 mL/min.
tuximab. Cautions: Preexisting IgE anti- Storage • Refrigerate vials. • Infu-
bodies to cetuximab, coronary artery dis- sion containers are stable for up to 12 hrs C
ease, HF, arrhythmias, pulmonary disease. if refrigerated, up to 8 hrs at room tem-
perature. • Discard unused portions.
ACTION
IV COMPATIBILITIES
Specifically binds to and inhibits epi-
dermal growth factor receptor (EGFR), Irinotecan (Camptosar).
blocking phosphorylation/activation of INDICATIONS/ROUTES/DOSAGE
receptor-associated kinases. Therapeu-
Head/Neck Cancer, Metastatic Colorectal
tic Effect: Inhibits tumor cell growth,
Cancer
inducing apoptosis (cell death).
IV: ADULTS, ELDERLY: Initially, 400 mg/
PHARMACOKINETICS m2 as a loading dose. Maintenance: 250
mg/m2 infused over 60 min wkly. Continue
Reaches steady-state levels by the third
until disease progression or unacceptable
wkly infusion. Clearance decreases as
toxicity.
dose increases. Half-life: 114 hrs
(range: 75–188 hrs). Dosage in Renal/Hepatic Impairment
No dose adjustment.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses placental SIDE EFFECTS
barrier; may cause fetal harm; abortifacient. Frequent (90%–25%): Acneiform rash,
Breastfeeding not recommended. Chil- malaise, fever, nausea, diarrhea, constipa-
dren: Safety and efficacy not established. tion, headache, abdominal pain, anorexia,
Elderly: No age-related precautions noted. vomiting. Occasional (16%–10%): Nail
disorder, back pain, stomatitis, peripheral
INTERACTIONS edema, pruritus, cough, insomnia. Rare
DRUG: None significant. HERBAL: None (9%–5%): Weight loss, depression, dys-
significant. FOOD: None known. LAB pepsia, conjunctivitis, alopecia.
VALUES: May decrease WBCs; serum
ADVERSE EFFECTS/TOXIC
calcium, magnesium, potassium.
REACTIONS
AVAILABILITY (Rx) Anemia occurs in 10% of pts. Severe infusion
Injection Solution: 2 mg/mL (50 mL, 100 reaction (rapid onset of airway obstruction,
mL). hypotension, severe urticaria) occurs rarely.
Dermatologic toxicity, pulmonary embolus,
ADMINISTRATION/HANDLING leukopenia, renal failure occur rarely.
IV NURSING CONSIDERATIONS
b ALERT c Do not give by IV push or BASELINE ASSESSMENT
bolus.
Monitor Hgb, Hct, serum potassium, mag-
Reconstitution • Does not require re-
nesium. Assess for evidence of anemia.
constitution. • Solution should appear
Question possibility of pregnancy. Ques-
clear, colorless; may contain a small
tion history of hypersensitivity reaction.
amount of visible, white particulates. • Do
not shake or dilute. • Infuse with a low INTERVENTION/EVALUATION
protein-binding 0.22-micron in-line filter. Monitor for evidence of infusion reaction
Rate of administration • First dose (rapid onset of bronchospasm, stridor,
should be given as a 120-min infu- hoarseness, urticaria, hypotension) during
sion. • Maintenance infusion should be infusion and for at least 1 hr postinfusion.
Canadian trade name Non-Crushable Drug High Alert drug
240 chlorambucil
Pts may experience first severe infusion sive drug regimen. Cautions: History of
reaction during later infusions. Assess skin bone marrow suppression, head trauma,
for evidence of dermatologic toxicity (de- hepatic impairment, nephrotic syndrome,
C velopment of inflammatory sequelae, dry seizure disorder; administration of live
skin, exfoliative dermatitis, rash). Monitor vaccines to immunocompromised pts.
CBC, serum electrolytes, acute onset or
worsening pulmonary symptoms. ACTION
Inhibits DNA, RNA synthesis by cross-
PATIENT/FAMILY TEACHING
linking with DNA strands. Therapeutic
• Do not have immunizations without Effect: Interferes with DNA replication
physician’s approval (drug lowers resis- and RNA transcription.
tance). • Avoid contact with anyone who
recently received a live virus vaccine. PHARMACOKINETICS
• Avoid crowds, those with i­nfection. Rapidly, completely absorbed from GI
• Wear sunscreen, limit sun exposure tract. Protein binding: 99%. Metabolized
(sunlight can exacerbate skin reac- in liver to active metabolite. Not removed
tions). • Avoid pregnancy. • Report by hemodialysis. Half-life: 1.5 hrs; me-
cardiac or lung symptoms, severe rash. tabolite, 2.5 hrs.
LIFESPAN CONSIDERATIONS
chlorambucil Pregnancy/Lactation: If possible, avoid
use during pregnancy, esp. first trimester.
klor-am-bue-sil Breastfeeding not recommended. Chil-
(Leukeran) dren: No age-related precautions noted.
j BLACK BOX ALERT j May When taken for nephrotic syndrome, may
cause myelosuppression. Affects increase risk of seizures. Elderly: No age-
fertility; potential for carcinogenic, related precautions noted.
mutagenic, teratogenic effects.
May cause azoospermia. INTERACTIONS
Do not confuse Leukeran with DRUG: May decrease therapeutic effect
Alkeran, Leukine, or Myleran. of BCG (intravesical), vaccines (live).
uCLASSIFICATION
May increase adverse effects of vaccines
(live). May increase myelosuppressive
PHARMACOTHERAPEUTIC: Alkylat- effect of myelosuppressants (e.g.,
ing agent, nitrogen mustard. CLINI- cladribine). HERBAL: Echinacea may
CAL: Antineoplastic. decrease effects. FOOD: Acidic foods,
spicy foods may delay absorption. LAB
USES VALUES: May increase serum alkaline
Treatment of chronic lymphocytic leuke- phosphatase, AST, uric acid.
mia (CLL), Hodgkin’s and non-Hodgkin’s AVAILABILITY (Rx)
lymphomas (NHL). OFF-LABEL: Nephrotic
Tablets: 2 mg.
syndrome in children, Waldenström’s
macroglobulinemia. ADMINISTRATION/HANDLING
PRECAUTIONS PO
Contraindications: Hypersensitivity to • Give 30–60 min before food.
chlorambucil. Previous allergic reaction INDICATIONS/ROUTES/DOSAGE
to other alkylating agents, prior resistance
Chronic Lymphocytic Leukemia (CLL)
to chlorambucil, pregnancy. Extreme Cau-
PO: ADULTS, ELDERLY: 0.1 mg/kg/day
tions: Treatment within 4 wks after full-
for 3–6 wks or 0.4 mg/kg pulsed doses
course radiation therapy or myelosuppres-

underlined – top prescribed drug


cinacalcet 241
administered intermittently, biweekly or INTERVENTION/EVALUATION
monthly (increased by 0.1 mg/kg/dose Monitor CBC, serum uric acid, LFT. Monitor
until response/toxicity observed). for hematologic toxicity (fever, sore throat,
signs of local infection, unusual bruis- C
Hodgkin’s Lymphoma (HL) ing/bleeding from any site), symptoms of
PO: ADULTS, ELDERLY: 0.2 mg/kg/day ­anemia (excessive fatigue, weakness). As-
for 3–6 wks. sess skin for rash, pruritus, urticaria.
Non-Hodgkin’s Lymphoma (NHL) PATIENT/FAMILY TEACHING
PO: ADULTS, ELDERLY: 0.1 mg/kg/day for
• Increase fluid intake (may protect against
3–6 wks. hyperuricemia). • Avoid acidic or spicy
Dosage in Renal Impairment foods; may delay absorption of medica-
CrCl 10–50 mL/min: 75% of dose. CrCl tion. • Do not have immunizations without
less than 10 mL/min: 50% of dose. physician’s approval (drug lowers resis-
tance). • Avoid contact with those who have
Dosage in Hepatic Impairment recently received live virus vac-
Use caution. cine. • Promptly report fever, sore throat,
signs of local infection, unusual bruising/
SIDE EFFECTS bleeding from any site, nausea, vomiting, rash.
Expected: GI effects (nausea, vomiting,
anorexia, diarrhea, abdominal distress),
generally mild, last less than 24 hrs, oc-
cur only if single dose exceeds 20 mg. cinacalcet
Occasional: Rash, dermatitis, pruritus,
oral ulcerations. Rare: Alopecia, urti- sin-a-kal-set
caria, erythema, hyperuricemia. (Sensipar)
uCLASSIFICATION
ADVERSE EFFECTS/TOXIC
REACTIONS PHARMACOTHERAPEUTIC: Calcium
Hematologic toxicity due to severe my- receptor agonist. CLINICAL: Calci-
elosuppression occurs frequently, mani- mimetic.
fested as neutropenia, anemia, throm-
bocytopenia. After discontinuation of USES
therapy, thrombocytopenia, neutropenia
usually last for 1–2 wks, but may per- Treatment of severe hypercalcemia in
sist for 3–4 wks. Neutrophil count may pts with primary parathyroid carcinoma.
continue to decrease for up to 10 days Treatment of secondary hyperparathy-
after last dose. Toxicity appears to be less roidism in pts with chronic renal dis-
severe with intermittent drug administra- ease on dialysis. Treatment of severe
tion. Overdosage may produce seizures hypercalcemia in pts with primary hy-
in children. Excessive serum uric acid perparathyroidism unable to undergo
level, hepatotoxicity occur rarely. parathyroidectomy.

NURSING CONSIDERATIONS PRECAUTIONS


Contraindications: Hypersensitivity to cina-
BASELINE ASSESSMENT calcet. Serum calcium lower than the lower
Obtain CBC before therapy and wkly dur- limit of normal range. Cautions: Cardio-
ing therapy, WBC count 3–4 days follow- vascular disease, moderate to severe he-
ing each wkly, CBC during first 3–6 wks patic impairment, seizure disorder.
of therapy (4–6 wks if pt on intermittent
dosing schedule).

Canadian trade name Non-Crushable Drug High Alert drug


242 cinacalcet

ACTION twice daily, 90 mg twice daily, and 90 mg


Increases sensitivity of calcium-sensing 3–4 times/day) every 2–4 wks as needed
receptor on parathyroid gland to ac- to normalize serum calcium level. Maxi-
C tivation by extracellular calcium, thus mum: 360 mg/day (as 90 mg 4 times/day).
lowering parathyroid hormone (PTH),
Secondary Hyperparathyroidism
calcium, and phosphorus levels. Thera-
PO: ADULTS, ELDERLY: Initially, 30 mg
peutic Effect: Prevents progressive bone
once daily. Titrate dosage sequentially (60,
disease and adverse effects associated
90, 120, and 180 mg once daily) every 2–4
with disorders of mineral metabolism.
wks to maintain iPTH level between 150
PHARMACOKINETICS and 300 pg/mL. Maximum: 180 mg/day.
Extensively distributed after PO adminis- Dosage in Renal Impairment
tration. Protein binding: 93%–97%. Me- No dose adjustment.
tabolized in liver. Excreted in urine (80%),
feces (15%). Half-life: 30–40 hrs. Dosage in Hepatic Impairment
Moderate to severe impairment:
LIFESPAN CONSIDERATIONS Use caution.
Pregnancy/Lactation: May cross pla-
cental barrier; unknown if distributed in SIDE EFFECTS
breast milk. Safe usage during lactation Frequent (31%–21%): Nausea, vomiting,
not established (potential adverse reac- diarrhea. Occasional (15%–10%): Myalgia,
tion in infants). Children: Safety and dizziness. Rare (7%–5%): Asthenia, hyper-
efficacy not established. Elderly: No tension, anorexia, noncardiac chest pain.
age-related precautions noted.
INTERACTIONS ADVERSE EFFECTS/TOXIC
REACTIONS
DRUG: Strong CYP3A4 inhibitors
(e.g., erythromycin, ketoconazole, Overdose may lead to hypocalcemia, sei-
ritonavir) increase concentration/effect. zures, worsening of HF.
May increase concentration/effect of thio-
ridazine. May decrease concentration/ NURSING CONSIDERATIONS
effect of tamoxifen. HERBAL: None sig- BASELINE ASSESSMENT
nificant. FOOD: High-fat meals increase
Establish baseline serum electrolyte lev-
plasma concentration. LAB VALUES: May
els (esp. serum calcium, phosphate, ion-
decrease serum calcium, phosphorus.
ized calcium).
AVAILABILITY (Rx) INTERVENTION/EVALUATION
Tablets: 30 mg, 60 mg, 90 mg. Monitor serum calcium, phosphate, ion-
ized calcium for hyperparathyroidism.
ADMINISTRATION/HANDLING Monitor daily pattern of bowel activity, stool
PO consistency. Obtain order for antidiarrhea,
• Store at room temperature. • Do not antiemetic medication to prevent serum
break, crush, dissolve, or divide film- electrolyte imbalance. Assess for evidence
coated tablets. • Administer with food of dizziness; institute fall risk precautions.
or shortly after a meal.
PATIENT/FAMILY TEACHING
INDICATIONS/ROUTES/DOSAGE • Take with food or shortly after a
Hypercalcemia in Parathyroid Carcinoma; meal. • Do not chew, crush, dissolve,
Primary Hyperparathyroidism or divide film-coated tablets. • Notify
PO: ADULTS, ELDERLY: Initially, 30 mg twice physician if vomiting, diarrhea, cramp-
daily. Titrate dosage sequentially (60 mg ing, muscle pain, numbness occurs.
underlined – top prescribed drug
ciprofloxacin 243
impairment, CNS disorders, seizures,
ciprofloxacin rheumatoid arthritis, history of QT pro-
longation, uncorrected hypokalemia,
sip-roe-flox-a-sin hypomagnesemia, myasthenia gravis. C
(Cetraxal, Ciloxan, Cipro, Cipro XR) Suspension not used through feeding or
j BLACK BOX ALERT jMay gastric tubes. Use in children (due to ad-
increase risk of tendonitis, tendon verse events to joints/surrounding tissue).
rupture. May exacerbate myasthe-
nia gravis. ACTION
Do not confuse Ciloxan with
Cytoxan, or Cipro with Ceftin, or Inhibits enzyme, DNA gyrase, in suscep-
ciprofloxacin with cephalexin. tible bacteria, interfering with bacte-
rial cell replication. Therapeutic Ef-
FIXED-COMBINATION(S) fect: Bactericidal.
Cipro HC Otic: ciprofloxacin/hydro- PHARMACOKINETICS
cortisone (a steroid): 0.2%/1%. Cip-
roDex Otic: ciprofloxacin/dexameth- Well absorbed from GI tract. Protein bind-
asone (a corticosteroid): 0.3%/0.1%. ing: 20%–40%. Widely distributed includ-
ing to CSF. Metabolized in liver. Primarily
uCLASSIFICATION excreted in urine. Minimal removal by
PHARMACOTHERAPEUTIC: Fluoro- hemodialysis. Half-life: 3–5 hrs (in-
quinolone. CLINICAL: Antibiotic. creased in renal impairment, elderly).
LIFESPAN CONSIDERATIONS
USES Pregnancy/Lactation: Unknown if
Treatment of susceptible infections due distributed in breast milk. If possible,
to E. coli, K. pneumoniae, E. cloacae, do not use during pregnancy/lactation
P. mirabilis, P. vulgaris, P. aeruginosa, (risk of arthropathy to fetus/infant).
H. influenzae, M. catarrhalis, S. pneu- Children: Arthropathy may occur. El-
moniae, S. aureus (methicillin suscep- derly: Age-related renal impairment
tible), S. epidermidis, S. pyogenes, C. may require dosage adjustment.
jejuni, Shigella spp., S. typhi including
intra-abdominal, bone, joint, lower respi- INTERACTIONS
ratory tract, skin/skin structure infections; DRUG: Antacids, calcium, magnesium,
UTIs, infectious diarrhea, prostatitis, si- zinc, iron preparations, sucralfate
nusitis, typhoid fever, febrile neutropenia. may decrease absorption. May increase
Ophthalmic: Treatment of superficial effects of caffeine, oral anticoagulants
ocular infections. Otic: Treatment of acute (e.g., warfarin). May increase concen-
otitis externa due to susceptible strains of tration/effect of pimozide, tizanidine.
P. aeruginosa or S. aureus. OFF-LABEL: May increase concentration, toxicity of
Treatment of chancroid. Acute pulmonary theophylline. HERBAL: Dong quai,
exacerbations in cystic fibrosis, dissemi- St. John’s wort may increase photo-
nated gonococcal infections, prophylaxis sensitization. FOOD: None known. LAB
to Neisseria meningitidis following close VALUES: May increase serum alkaline
contact with infected person. Infectious phosphatase, creatine kinase (CK), LDH,
diarrhea (children); periodontitis. ALT, AST.
PRECAUTIONS AVAILABILITY (Rx)
Contraindications: Hypersensitivity to 200 mg/100 mL,
Infusion, Solution:
ciprofloxacin, other quinolones. Concur- 400 mg/200 mL. Ophthalmic Ointment:
rent use of tiZANidine. Cautions: Renal (Ciloxan): 0.3%. Ophthalmic Solution:

Canadian trade name Non-Crushable Drug High Alert drug


244 ciprofloxacin
(Ciloxan):0.3%. Otic Solution: (Cetraxal): IV COMPATIBILITIES
0.2% (single-dose container: 0.25 mL). Calcium gluconate, diltiaZEM (Cardi-
Suspension, Oral: 250 mg/5 mL, 500 zem), DOBUTamine (Dobutrex), DO-
C mg/5 mL. Tablets: 100 mg, 250 mg, 500 Pamine (Intropin), lidocaine, LORaz-
mg, 750 mg. epam (Ativan), magnesium, midazolam
Tablets (Extended-Release): 500 (Versed), potassium chloride.
mg, 1,000 mg.
INDICATIONS/ROUTES/DOSAGE
ADMINISTRATION/HANDLING Note: Not recommended as first choice
IV in pregnancy/lactation or in children
younger than 18 yrs due to adverse events
Reconstitution • Available prediluted related to joints/surrounding tissue.
in infusion container ready for use. Final
concentration not to exceed 2 mg/mL. Usual Dosage Range
Rate of administration • Infuse over PO: ADULTS, ELDERLY: 250–750 mg q12h.
60 min (reduces risk of venous irritation). 10
CHILDREN: Mild to moderate infections:
Storage • Store at room tempera- mg/kg twice daily. Maximum: 500 mg/
ture. • Solution appears clear, color- dose. Severe infections: 15–20 mg/kg
less to slightly yellow. twice daily. Maximum: 750 mg/dose.
IV: ADULTS, ELDERLY: 200–400 mg
PO q12h. CHILDREN: 10 mg/kg q8–12h.
• May be given with food to minimize GI Maximum: 400 mg/dose.
upset. • Give at least 2 hrs before or 6
hrs after antacids, calcium, iron, zinc- Usual Ophthalmic Dosage
containing products. • Do not adminis- ADULTS, ELDERLY, CHILDREN: (Solu-
ter suspension through feeding or gastric tion): 1–2 drops q2h while awake
tubes. • NG tube: Crush immediate- for 2 days, then 1–2 drops q4h while
release tablet and mix with water. Flush awake for 5 days. (Ointment): Apply 3
tube before/after administration. times/day for 2 days, then 2 times/day for
5 days.
Ophthalmic
• Place gloved finger on lower eyelid and Usual Otic Dosage
pull out until a pocket is formed between ADULTS, ELDERLY, CHILDREN: Otic solu-
eye and lower lid. • Place ointment or tion 0.2%. Instill 0.25 mL (0.5 mg) 2
drops into pocket. • Instruct pt to close times/day for 7 days.
eye gently for 1–2 min (so that medication
will not be squeezed out of the sac). • In- Dosage in Renal Impairment
struct pt using ointment to roll eyeball to Dosage and frequency are modified
increase contact area of drug to eye. • In- based on creatinine clearance and the
struct pt using solution to apply digital pres- severity of the infection.
sure to lacrimal sac at inner canthus for 1 Creatinine Clearance Dosage
min to minimize systemic absorption. • Do Immediate-Release
not use ophthalmic solution for injection. 30–50 mL/min PO: 250–500 mg
q12h
IV INCOMPATIBILITIES 5–29 mL/min 250–500 mg q18h
ESRD, HD, PD 250–500 mg q24h
Ampicillin and sulbactam (Unasyn), Extended-Release
cefepime (Maxipime), dexamethasone < 30 mL/min 500 mg q24h
(Decadron), furosemide (Lasix), hepa- ESRD, HD, PD 500 mg q24h
rin, hydrocortisone (Solu-Cortef), meth- IV 5–29 mL/min 200–400 mg
ylPREDNISolone (Solu-Medrol), pheny- q18–24h
toin (Dilantin), sodium bicarbonate.

underlined – top prescribed drug


CISplatin 245
Dosage in Hepatic Impairment PATIENT/FAMILY TEACHING
No dose adjustment. • Do not skip doses; take full course of
therapy. • Maintain adequate hydration
SIDE EFFECTS to prevent crystalluria. • Do not take C
Frequent (5%–2%): Nausea, diarrhea, antacids within 2 hrs of ciprofloxacin
dyspepsia, vomiting, constipation, flatu- (reduces/destroys effectiveness). •
lence, confusion, crystalluria. Ophthal- Shake suspension well before using; do
mic: Burning, crusting in corner of eye. not chew microcapsules in suspen-
Occasional (less than 2%): Abdominal sion. • Sugarless gum, hard candy may
pain/discomfort, headache, rash. Oph- relieve bad taste. • Avoid caffeine. •
thalmic: Altered taste, sensation of for- Report tendon pain or swelling. • Avoid
eign body in eye, eyelid redness, itching. exposure to sunlight/artificial light (may
Rare (less than 1%): Dizziness, confusion, cause photosensitivity reaction). • Re-
tremors, hallucinations, hypersensitivity re- port persistent diarrhea.
action, insomnia, dry mouth, paresthesia.
ADVERSE EFFECTS/TOXIC
REACTIONS CISplatin
Superinfection (esp. enterococcal, fun-
gal), nephropathy, cardiopulmonary sis-pla-tin
arrest, cerebral thrombosis may occur. j BLACK BOX ALERT jCumula-
Hypersensitivity reaction (rash, pruritus, tive renal toxicity may be severe.
blisters, edema, burning skin), photo- Dose-related toxicities include my-
sensitivity have occurred. Sensitization elosuppression, nausea, vomiting.
to ophthalmic form may contraindicate Ototoxicity, especially pronounced
in children, noted by tinnitus, loss of
later systemic use of ciprofloxacin. May high-frequency hearing, deafness.
exacerbate muscle weakness in pts with Must be administered by personnel
myasthenia gravis. Dermatologic condi- trained in administration/handling
tions such as toxic epidermal necrolysis, of chemotherapeutic agents.
Stevens-Johnson syndrome have been Anaphylactic reaction can occur
within minutes of administration.
reported. Cases of severe hepatotoxicity Avoid confusion between CISplatin
have occurred. May increase risk of ten- and CARBOplatin.
donitis, tendon rupture. Do not confuse CISplatin with
CARBOplatin or oxaliplatin.
NURSING CONSIDERATIONS
uCLASSIFICATION
BASELINE ASSESSMENT
Question for history of hypersensitivity PHARMACOTHERAPEUTIC: Alkylat-
to ciprofloxacin, quinolones; myasthenia ing agent. CLINICAL: Antineoplastic.
gravis, renal/hepatic impairment.
INTERVENTION/EVALUATION USES
Obtain urinalysis for microscopic analy- Treatment of metastatic testicular can-
sis for crystalluria prior to and dur- cers, metastatic ovarian cancers, ad-
ing treatment. Evaluate food tolerance. vanced bladder cancer. OFF-LABEL:
Monitor daily pattern of bowel activity, Breast, cervical, endometrial, esopha-
stool consistency. Encourage hydration geal, gastric, head and neck, lung (small-
(reduces risk of crystalluria). Monitor cell, non–small-cell) carcinomas; Hodg-
for dizziness, headache, visual changes, kin’s and non-Hodgkin’s lymphomas;
tremors. Assess for chest, joint pain. malignant melanoma, neuroblastoma,
Ophthalmic: Observe therapeutic re- osteosarcoma, soft tissue sarcoma,
sponse. Wilms’ tumor.

Canadian trade name Non-Crushable Drug High Alert drug


246 CISplatin

PRECAUTIONS mutagenic, teratogenic. Handle with


Contraindications: Hypersensitivity to extreme care during preparation/admin-
CISplatin. Hearing impairment, myelosup- istration.
C pression, preexisting renal impairment. IV
Cautions: Elderly, renal impairment.
Dilution • Dilute desired dose in
ACTION 250–1,000 mL 0.9% NaCl, D5/0.45%
Inhibits DNA synthesis by cross-linking NaCl, or D5/0.9% NaCl to concentra-
with DNA strands. Cell cycle–phase non- tion of 0.05–2 mg/mL. Solution should
specific. Therapeutic Effect: Prevents have final NaCl concentration of 0.2% or
cellular division. greater.
Rate of administration • Infuse over
PHARMACOKINETICS 6–8 hrs (per protocol). • Avoid rapid
Widely distributed. Protein binding: infusion (increases risk of nephrotoxic-
greater than 90%. Undergoes rapid ity, ototoxicity). • Monitor for anaphy-
nonenzymatic conversion to inactive me- lactic reaction during first few minutes of
tabolite. Excreted in urine. Removed by infusion.
hemodialysis. Half-life: 58–73 hrs (in- Storage • Protect from sunlight. •
creased in renal impairment). Do not refrigerate (may precipitate). Dis-
card if precipitate forms. IV infusion:
LIFESPAN CONSIDERATIONS Stable for 72 hrs at 39°F–77°F.
Pregnancy/Lactation: If possible,
avoid use during pregnancy, esp. first tri- IV INCOMPATIBILITIES
mester. Breastfeeding not recommended. Amphotericin B complex (Abelcet, AmBi-
Children: Ototoxic effects may be more some, Amphotec), cefepime (Maxip-
severe. Elderly: Age-related renal im- ime), piperacillin and tazobactam (Zo-
pairment may require dosage adjustment. syn), sodium bicarbonate.

INTERACTIONS IV COMPATIBILITIES
DRUG: Bone marrow depressants Etoposide (VePesid), granisetron (Ky-
(e.g., PACLitaxel) may increase my- tril), heparin, HYDROmorphone (Di-
elosuppression. Live virus vaccines laudid), lipids, LORazepam (Ativan),
may potentiate virus replication, in- magnesium sulfate, mannitol, mor-
crease vaccine side effects, decrease phine, ondansetron (Zofran), palono-
pt’s antibody response to vaccine. setron (Aloxi).
HERBAL: Echinacea may decrease
effects. FOOD: None known. LAB VAL- INDICATIONS/ROUTES/
UES: May increase serum BUN, creati-
DOSAGE
nine, uric acid, AST. May decrease CrCl, Note: Pretreatment hydration with 1–2
serum calcium, magnesium, phosphate, liters of fluid recommended. Adequate
potassium, sodium. May cause positive hydration, urine output greater than
Coombs’ test. 100 mL/hr should be maintained for
24 hrs after administration. Verify any
AVAILABILITY (Rx) cisplatin dose exceeding 100 mg/m2/
Injection Solution: 1 mg/mL (50 mL, 100 course.
mL, 200 mL).
Bladder Cancer
ADMINISTRATION/HANDLING (Single agent):
IV: ADULTS, ELDERLY:
b ALERT c Wear protective gloves 50–70 mg/m2 q3–4wks.
during handling. May be carcinogenic,

underlined – top prescribed drug


citalopram 247
Ovarian Cancer
NURSING CONSIDERATIONS
IV: ADULTS, ELDERLY: 75–100 mg/m2
q3–4wks (combination therapy) or 100 BASELINE ASSESSMENT
mg/m2 q4wks (single agent). Obtain baseline CBC, BMP, LFT. Pts C
should be well hydrated before and 24
Testicular Cancer
hrs after medication to ensure adequate
IV: ADULTS, ELDERLY: 20 mg/m2 daily urinary output (100 mL/hr), decrease
for 5 days repeated q3wks (in combina- risk of nephrotoxicity.
tion with bleomycin and etoposide).
INTERVENTION/EVALUATION
Dosage in Renal Impairment
Dosage is modified based on CrCl, BUN. Measure all emesis, urine output (general
b ALERT c Repeated courses of CISpla-
guideline requiring immediate notifica-
tin should not be given until serum cre- tion of physician: 750 mL/8 hrs, urinary
atinine is less than 1.5 mg/100 mL and/ output less than 100 mL/hr). Monitor
or BUN is less than 25 mg/100 mL. I&O q1–2h beginning with pretreatment
hydration, continue for 48 hrs after dose.
Creatinine Clearance Dosage
Assess vital signs q1–2h during infusion.
10–50 mL/min 75% of normal dose
Monitor urinalysis, serum electrolytes,
Less than 10 mL/min 50% of normal dose
Hemodialysis 50% of dose post LFT, renal function tests, CBC, platelet
dialysis count for changes from baseline.
Peritoneal dialysis 50% of dose
PATIENT/FAMILY TEACHING
Continuous renal re- 75% of dose
placement therapy • Report signs of ototoxicity (tinnitus,
hearing loss). • Do not have immuni-
Dosage in Hepatic Impairment zations without physician’s approval
No dose adjustment. (lowers body’s resistance). • Avoid
contact with those who have recently
SIDE EFFECTS taken oral polio vaccine. • Report if
Frequent: Nausea, vomiting (occurs in nausea/vomiting continues at
more than 90% of pts, generally beginning home. • Report signs of peripheral
1–4 hrs after administration and lasting up neuropathy.
to 24 hrs); myelosuppression (affecting
25%–30% of pts, with recovery generally
occurring in 18–23 days). Occasional: Pe-
ripheral neuropathy (with prolonged ther- citalopram
apy [4–7 mos]). Pain/redness at injection
site, loss of taste, appetite. Rare: Hemolytic sye-tal-o-pram
anemia, blurred vision, stomatitis. (CeleXA)
ADVERSE EFFECTS/TOXIC j BLACK BOX ALERT jIncreased
risk of suicidal thinking and behav-
REACTIONS ior in children, adolescents, young
Anaphylactic reaction (angioedema, adults 18–24 yrs with major depres-
wheezing, tachycardia, hypotension) may sive disorder, other psychiatric
disorders.
occur in first few minutes of administra- Do not confuse CeleXA with
tion in pt previously exposed to CISplatin. CeleBREX, Cerebyx, Ranexa, or
Nephrotoxicity occurs in 28%–36% of pts ZyPREXA.
treated with a single dose, usually during
second wk of therapy. Ototoxicity (tin- uCLASSIFICATION
nitus, hearing loss) occurs in 31% of pts PHARMACOTHERAPEUTIC: Selective
treated with a single dose (more severe in serotonin reuptake inhibitor. CLINI-
children). Symptoms may become more CAL: Antidepressant.
frequent, severe with repeated doses.
Canadian trade name Non-Crushable Drug High Alert drug
248 citalopram

USES phenelzine, selegiline), triptans may


Treatment of unipolar major depression. cause serotonin syndrome (excitement,
OFF-LABEL: Treatment of alcohol abuse, diaphoresis, rigidity, hyperthermia, au-
C diabetic neuropathy, obsessive-compul- tonomic hyperactivity, coma). Strong
sive disorder, smoking cessation, GAD, CYP3A4 inducers (e.g., carBAMaze-
panic disorder. pine, phenytoin, rifAMPin) may de-
crease concentration/effect. HERBAL: St.
PRECAUTIONS John’s wort may decrease concentra-
Contraindications: Hypersensitivity to tion/effect. FOOD: None known. LAB
citalopram, use of MAOIs intended to VALUES: May decrease serum sodium.
treat psychiatric disorders (concurrently
AVAILABILITY (Rx)
or within 14 days of discontinuing either
citalopram or MAOI), initiation in pts re- Oral Solution: 10 mg/5 mL. Tablets: 10
ceiving linezolid or methylene blue. Con- mg, 20 mg, 40 mg.
current use with pimozide. Cautions: El-
ADMINISTRATION/HANDLING
derly, hepatic/renal impairment, seizure
disorder. Not recommended in pts with PO
congenital long QT syndrome, bradycar- • Give without regard to food.
dia, recent MI, uncompensated HF, hypo-
INDICATIONS/ROUTES/DOSAGE
kalemia, or hypomagnesemia; pts at high
risk of suicide. Note: Doses greater than 40 mg not rec-
ommended.
ACTION
Depression
Blocks uptake of the neurotransmitter
PO: ADULTS YOUNGER THAN 60 YRS: Ini-
serotonin at CNS presynaptic neuronal
tially, 20 mg once daily in the morning
membranes, increasing its availability at
or evening. May increase in 20-mg in-
postsynaptic receptor sites. Therapeutic
crements at intervals of no less than 1
Effect: Relieves symptoms of depression.
wk. Maximum: 40 mg/day. ELDERLY 60
PHARMACOKINETICS YRS OR OLDER: 20 mg once daily. Maxi-
mum: 20 mg/day.
Well absorbed after PO administration.
Protein binding: 80%. Extensively metab- Dose Modification
olized in liver. Excreted in urine. Half- Hepatic impairment; poor metabo-
life: 35 hrs. lizers of CYP2C19; concomitant use
of CYP2C19 inhibitors: 20 mg once
LIFESPAN CONSIDERATIONS daily. Maximum: 20 mg/day.
Pregnancy/Lactation: Distributed in
breast milk. Children: May cause in- Dosage in Renal Impairment
creased anticholinergic effects, hyperex- Mild to moderate impairment: No
citability. Elderly: More sensitive to anti- dose adjustment. Severe impairment:
cholinergic effects (e.g., dry mouth), more Use caution.
likely to experience dizziness, sedation,
confusion, hypotension, hyperexcitability. SIDE EFFECTS
Frequent (21%–11%): Nausea, dry mouth,
INTERACTIONS drowsiness, insomnia, diaphoresis. Oc-
DRUG: CYP2C19 inhibitors (e.g., flu- casional (8%–4%): Tremor, diarrhea,
conazole), other medications pro- abnormal ejaculation, dyspepsia, fa-
longing QT interval (e.g., amioda- tigue, anxiety, vomiting, anorexia. Rare
rone, azithromycin, ciprofloxacin, (3%–2%): Sinusitis, sexual dysfunction,
haloperidol) may increase risk of QT menstrual disorder, abdominal pain, agi-
prolongation. Linezolid, MAOIs (e.g., tation, decreased libido.
underlined – top prescribed drug
clarithromycin 249

ADVERSE EFFECTS/TOXIC USES


REACTIONS Treatment of susceptible infections due to
Overdose manifested as dizziness, C. pneumoniae, H. influenzae, H. para-
drowsiness, tachycardia, confusion, sei- influenzae, H. pylori, M. catarrhalis, C
zures, torsades de pointes, ventricular M. avium, M. pneumoniae, S. aureus,
tachycardia, sudden death. Serotonin S. pneumoniae, S. pyogenes, including
syndrome or neuroleptic malignant syn- bacterial exacerbation of bronchitis, otitis
drome (NMS)–like reactions have been media, acute maxillary sinusitis, Mycobac-
reported. terium avium complex (MAC), pharyn-
gitis, tonsillitis, H. pylori duodenal ulcer,
NURSING CONSIDERATIONS community-acquired pneumonia, skin and
BASELINE ASSESSMENT soft tissue infections. Prevention of MAC
disease. OFF-LABEL: Prophylaxis of infec-
Hepatic/renal function tests, blood tive endocarditis, pertussis, Lyme disease.
counts should be performed periodically
for pts on long-term therapy. Observe, PRECAUTIONS
record behavior. Assess psychological Contraindications: Hypersensitivity to
status, thought content, sleep pattern, clarithromycin, other macrolide antibi-
appearance, interest in environment. otics. History of QT prolongation or ven-
Screen for bipolar disorder. tricular arrhythmias, including torsades
INTERVENTION/EVALUATION de pointes. History of cholestatic jaundice
Supervise suicidal-risk pt closely during or hepatic impairment with prior use of
early therapy (as depression lessens, en- clarithromycin. Concomitant use with
ergy level improves, increasing suicide colchicine (in pts with renal/hepatic im-
potential). Assess appearance, behavior, pairment), statins, pimozide, ergotamine,
speech pattern, level of interest, mood. dihydroergotamine. Cautions: Hepatic/
renal impairment, elderly with severe
PATIENT/FAMILY TEACHING renal impairment, myasthenia gravis,
• Do not stop taking medication or in- coronary artery disease. Pts at risk of
crease dosage. • Avoid alco- prolonged cardiac repolarization. Avoid
hol. • Avoid tasks that require alert- use with uncorrected electrolytes (e.g.,
ness, motor skills until response to drug hypokalemia, hypomagnesemia), clini-
is established. • Report worsening de- cally significant bradycardia, class IA or
pression, suicidal ideation, unusual III antiarrhythmics (see Classification).
changes in behavior.
ACTION
Binds to ribosomal receptor sites of sus-
ceptible organisms, inhibiting protein
clarithromycin synthesis of bacterial cell wall. Thera-
peutic Effect: Bacteriostatic; may be
kla-rith-roe-mye-sin bactericidal with high dosages or very
(Apo-Clarithromycin , PMS- susceptible microorganisms.
Clarithromycin )
Do not confuse clarithromycin PHARMACOKINETICS
with Claritin, clindamycin, or Well absorbed from GI tract. Protein bind-
erythromycin. ing: 65%–75%. Widely distributed (except
CNS). Metabolized in liver. Primarily ex-
uCLASSIFICATION
creted in urine. Not removed by hemodi-
PHARMACOTHERAPEUTIC: Mac- alysis. Half-life: 3–7 hrs; metabolite,
rolide. CLINICAL: Antibiotic. 5–9 hrs (increased in renal impairment).

Canadian trade name Non-Crushable Drug High Alert drug


250 clarithromycin

LIFESPAN CONSIDERATIONS twice daily. HD: Administer dose after


Pregnancy/Lactation: Unknown if dis- dialysis complete.
tributed in breast milk. Children: Safety
C Combination with Atazanavir or Ritonavir
and efficacy not established in pts younger
than 6 mos. Elderly: Age-related renal im- CrCl 30–60 Decrease dose by 50%
mL/min
pairment may require dosage adjustment. CrCl less than Decrease dose by 75%
30 mL/min
INTERACTIONS
DRUG: May increase concentration/effects Dosage in Hepatic Impairment
of acalabrutinib, ado-trastuzumab, No dose adjustment.
axitinib, bosutinib, budesonide,
eletriptan, lovastatin. May increase SIDE EFFECTS
QT-prolonging effects of dronedarone. Occasional (6%–3%): Diarrhea, nausea,
HERBAL: St. John’s wort may decrease altered taste, abdominal pain. Rare (2%–
plasma concentration. FOOD: None 1%): Headache, dyspepsia.
known. LAB VALUES: May increase serum
BUN, ALT, AST, alkaline phosphatase, LDH, ADVERSE EFFECTS/TOXIC
creatinine, PT. May decrease WBC. REACTIONS
Antibiotic-associated colitis, other super-
AVAILABILITY (Rx) infections (abdominal cramps, severe
Oral Suspension: 125 mg/5 mL, 250 watery diarrhea, fever) may result from
mg/5 mL. Tablets: 250 mg, 500 mg. altered bacterial balance in GI tract.
Tablets (Extended-Release): 500 mg. Hepatotoxicity, thrombocytopenia occur
rarely.
ADMINISTRATION/HANDLING
PO NURSING CONSIDERATIONS
• Give immediate-release tablets, oral BASELINE ASSESSMENT
suspension without regard to
food. • Give q12h (rather than twice Question pt for allergies to clarithromy-
daily). • Shake suspension well before cin, erythromycins.
each use. • Extended-release tablets INTERVENTION/EVALUATION
should be given with food. • Do not Monitor daily pattern of bowel activity,
break, crush, dissolve, or divide ex- stool consistency. Mild GI effects may
tended-release tablets. be tolerable, but increasing severity may
INDICATIONS/ROUTES/DOSAGE indicate onset of antibiotic-associated
colitis. Be alert for superinfection: fever,
Usual Dosage Range vomiting, diarrhea, anal/genital pruritus,
PO: ADULTS, ELDERLY: 250–500 mg oral mucosal changes (ulceration, pain,
q12h or 1,000 mg once daily (2 × erythema).
500-mg extended-release tablets). CHIL-
DREN 6 MOS AND OLDER: (Immediate- PATIENT/FAMILY TEACHING
Release):7.5 mg/kg q12h. Maxi- • Continue therapy for full length of
mum: 500 mg/dose. treatment. • Doses should be evenly
spaced. • Biaxin may be taken without
Dosage in Renal Impairment regard to food. Take Biaxin XL with
CrCl less than 30 mL/min: Reduce food. • Report severe diarrhea.
dose by 50% and administer once or

underlined – top prescribed drug


clevidipine 251
uterine contractions during labor and de-
clevidipine livery. Children: Safety and efficacy not
established. Elderly: Start at low end of
clev-eye-di-peen dosing range. May experience greater hy- C
(Cleviprex) potensive effect.
Do not confuse clevidipine with
amlodipine, cladribine, clofara- INTERACTIONS
bine, clozapine, or Cleviprex DRUG: None significant. HERBAL: Herbs
with Claravis. with hypotensive properties (e.g., gar-
lic, ginger, hawthorn) may enhance
uCLASSIFICATION
effect. Yohimbe may decrease effect.
PHARMACOTHERAPEUTIC: Dihydro- FOOD: None known. LAB VALUES: May
pyridine calcium channel blocker. increase serum BUN, potassium, triglycer-
CLINICAL: Antihypertensive. ides, uric acid.
AVAILABILITY (Rx)
USES
50 mL (0.5 mg/mL),
Injection, Emulsion:
Management of hypertension when oral 100 mL (0.5 mg/mL).
therapy is not feasible or not desirable.
ADMINISTRATION/HANDLING
PRECAUTIONS
Contraindications: Hypersensitivity to IV
clevidipine. Allergy to soy or egg prod- Preparation • Do not dilute. • To
ucts; abnormal lipid metabolism (e.g., ensure uniformity of emulsion, gently
acute pancreatitis, lipoid nephrosis, invert vial several times before
pathologic hyperlipidemia if accompa- use. • Visually inspect for particulate
nied by hyperlipidemia), severe aortic matter or discoloration. Emulsion
stenosis. Cautions: HF; pt with disorders should appear milky white. Discard if
of lipid metabolism. discoloration or particulate matter is
ACTION observed.
Rate of administration • Titrate to
Causes potent arterial vasodilation by desired effect using infusion pump via
inhibiting the influx of calcium during peripheral or central line.
depolarization in arterial smooth mus- Storage • Refrigerate unused vial in
cle. Therapeutic Effect: Decreases original carton. • May store at con-
mean arterial pressure (MAP) by reduc- trolled room temperature (77°F) for up
ing systemic vascular resistance. to 2 mos. • Do not freeze. • Do not
PHARMACOKINETICS return to refrigerator once warmed to
room temperature. Once the stopper is
Widely and rapidly distributed. Full recov- punctured, use within 12 hrs. • Dis-
ery of therapeutic B/P occurs 5–15 min. card unused portions.
after discontinuation. Onset of effects: 2–4
min. Metabolized via hydrolysis by ester- IV INCOMPATIBILITIES
ases in blood and extravascular tissue. May be administered with, but not diluted
Protein binding: 99.5%. Excreted in urine in, solutions including Sterile Water for
(74%), feces (22%). Half-life: 15 min. Injection, 0.9% NaCl, dextrose-containing
LIFESPAN CONSIDERATIONS solutions, lactated Ringer’s, 10% amino
acid. Do not administer with other medi-
Pregnancy/Lactation: Unknown if cations.
distributed in breast milk. May depress

Canadian trade name Non-Crushable Drug High Alert drug


252 clindamycin

INDICATIONS/ROUTES/DOSAGE products, eggs products. Assess B/P, api-


Note: Individualize dosage depending cal pulse immediately before initiation.
on desired B/P and pt response. See man- INTERVENTION/EVALUATION
C ufacturer guidelines for dose conversion.
Monitor B/P, pulse rate. Generally, an in-
Hypertension crease of 1–2 mg/hour will produce an
IV: ADULTS, ELDERLY: Initiate infusion at additional 2–4 mm Hg decrease in systolic
1–2 mg/hr. Titration: Initially, dosage B/P. If an oral antihypertensive is required
may be doubled at short (90-sec) inter- to wean off infusion, consider the delay of
vals. As B/P approaches goal, an increase onset of oral medication’s effect. Pts who
in dosage should be less than double, receive prolonged IV infusions and are not
and time intervals between dose adjust- changed to other antihypertensives should
ments should be lengthened to q5–10 be monitored for rebound hypertension
min. Maintenance: Desired therapeu- for at least 8 hrs after discontinuation. Ob-
tic effect generally occurs at a rate of 4–6 tain serum triglyceride level in pts receiv-
mg/hr (pts with severe hypertension may ing prolonged infusions. Monitor for atrial
require limited doses up to 32 mg/hr). fibrillation, hypotension, reflex tachycar-
Maximum: 16 mg/hr (no more than 21 dia; exacerbation of HF in pts with history
mg/hr or 1000 mL is recommended per of HF. Beta blockers should be discontin-
24 hrs due to lipid load). ued only after a gradual reduction in dose.
Dosage in Renal Impairment PATIENT/FAMILY TEACHING
No dose adjustment. • In some pts, an oral blood pressure
medication may need to be started; com-
Dosage in Hepatic Impairment pliance is essential to control high blood
Not specified; use caution. pressure. • Life-threatening high blood
pressure crisis may occur up to 8 hrs
SIDE EFFECTS after stopping infusion; report severe
Occasional (6%–3%): Headache, insom- anxiety, chest pain, difficulty breathing,
nia, nausea, vomiting. Rare (less than headache, stroke-like symptoms (confu-
1%): Syncope, dyspnea. sion, difficulty speaking, paralysis, one-
sided weakness, vision loss).
ADVERSE EFFECTS/TOXIC
REACTIONS
May cause atrial fibrillation, hypoten- clindamycin
sion, reflex tachycardia. Rebound hy-
pertension may occur in pts who are not klin-da-mye-sin
transitioned to oral antihypertensives (Cleocin, Cleocin T, Clindagel,
after discontinuation. Dihydropyridine Clindesse)
calcium channel blockers are known to j BLACK BOX ALERT jMay
have negative inotropic effects, which cause severe, potentially fatal colitis
characterized by severe, persistent
may exacerbate HF. Rebound hyperten- diarrhea, severe abdominal cramps,
sion may cause emergent hypertensive passage of blood and mucus.
crisis, which may cause CVA, myocardial Do not confuse Cleocin with
infarction, renal failure, HF, seizures. Clinoril or Cubicin, or clin-
damycin with clarithromycin,
NURSING CONSIDERATIONS Claritin, or vancomycin.
BASELINE ASSESSMENT
uCLASSIFICATION
Screen for history of defective lipid me-
PHARMACOTHERAPEUTIC: Lincosa-
tabolism, pancreatitis, hypertriglyceride-
mia, severe aortic stenosis; allergy to soy mide. CLINICAL: Antibiotic.

underlined – top prescribed drug


clindamycin 253

USES in pts younger than 1 mo. Elderly: No


age-related precautions noted.
Systemic: Treatment of aerobic gram-
positive staphylococci and streptococci INTERACTIONS C
(not enterococci), Fusobacterium,
DRUG: None significant. HERBAL: St.
Bacteroides spp., and Actinomyces
John’s wort may decrease concentra-
for treatment of respiratory tract infec-
tion/effect. FOOD: None known. LAB
tions, skin/soft tissue infections, sepsis,
VALUES: May increase serum alkaline
intra-abdominal infections, infections of
phosphatase, ALT, AST.
female pelvis and genital tract, bacte-
rial endocarditis prophylaxis for dental AVAILABILITY (Rx)
and upper respiratory procedures in
penicillin-allergic pts, perioperative Capsules: 75 mg, 150 mg, 300 mg.
prophylaxis. Topical: Treatment of Cream, Vaginal: 2%. Gel, Topical: 1%.
acne vulgaris. Intravaginal: Treat- Infusion, Premix: 300 mg/50 mL, 600
ment of bacterial vaginosis. OFF-LABEL: mg/50 mL, 900 mg/50 mL. Injection
Treatment of actinomycosis, babesiosis, Solution: 150 mg/mL. Lotion: 1%. Oral
erysipelas, malaria, otitis media, Pneu- Solution: 75 mg/5 mL. Suppositories,
mocystis jiroveci pneumonia (PCP), Vaginal: 100 mg. Swabs, Topical: 1%.
sinusitis, toxoplasmosis. PO: Bacterial
vaginosis.
ADMINISTRATION/HANDLING
IV
PRECAUTIONS
Reconstitution • Dilute 300–600 mg
Contraindications: Hypersensitivity to with 50 mL D5W or 0.9% NaCl (900–
clindamycin. Cautions: Severe hepatic 1,200 mg with 100 mL).
dysfunction; history of GI disease (espe- Rate of administration • Infuse over
cially colitis). at least 10–60 min at rate not exceeding
30 mg/min. Severe hypotension, cardiac
ACTION arrest can occur with rapid administra-
Inhibits protein synthesis of bacterial cell tion. • No more than 1.2 g should be
wall by binding to bacterial ribosomal given in a single infusion.
receptor sites. Topically, decreases fatty Storage • Reconstituted IV infusion
acid concentration on skin. Therapeu- (piggyback) is stable for 16 days at room
tic Effect: Bacteriostatic or bacterio- temperature, 32 days if refrigerated.
cidal.
IM
PHARMACOKINETICS • Do not exceed 600 mg/dose. • Ad-
minister deep IM.
Rapidly absorbed from GI tract. Protein
binding: 92%–94%. Widely distributed. PO
Metabolized in liver. Primarily excreted • Store capsules at room tempera-
in urine. Not removed by hemodialysis. ture. • After reconstitution, oral solution
Half-life: 1.6–5.3 hrs (increased in is stable for 2 wks at room tempera-
renal/hepatic impairment, premature ture. • Do not refrigerate oral solu-
infants). tion (avoids thickening). • Give with at
least 8 oz water (minimizes esophageal ul-
LIFESPAN CONSIDERATIONS ceration). • Give without regard to food.
Pregnancy/Lactation: Readily crosses
placenta. Distributed in breast milk. Topical
Topical/Vaginal: Unknown if distrib- • Wash skin; allow to dry completely be-
uted in breast milk. Children: Caution fore application. • Shake topical lotion

Canadian trade name Non-Crushable Drug High Alert drug


254 clindamycin
well before each use. • Apply liquid, once daily as single dose in nonpregnant
solution, or gel in thin film to affected pts. Suppository: ADULTS: Once daily into
area. • Avoid contact with eyes or vagina at bedtime for 3 days.
C abraded areas.
Acne Vulgaris
Vaginal, Cream or Suppository Topical: ADULTS: Apply thin layer to af-
• Use one applicatorful or suppository fected area twice daily (pledget, lotion,
at bedtime. • Fill applicator that solution); once daily (gel, foam).
comes with cream or suppository to in-
dicated level. • Instruct pt to lie on Dosage in Renal/Hepatic Impairment
back with knees drawn upward and No dose adjustment.
spread apart. • Insert applicator into
vagina and push plunger to release SIDE EFFECTS
medication. • Withdraw, wash appli- Frequent: Systemic: Abdominal pain,
cator with soap and warm wa- nausea, vomiting, diarrhea. Topical: Dry,
ter. • Wash hands promptly to avoid scaly skin. Vaginal: Vaginitis, pruritus.
spreading infection. Occasional: Systemic: Phlebitis; pain,
induration at IM injection site; allergic
IV INCOMPATIBILITIES reaction, urticaria, pruritus. Topical:
Allopurinol (Aloprim), fluconazole (Di- Contact dermatitis, abdominal pain, mild
flucan). diarrhea, burning, stinging. Vaginal:
Headache, dizziness, nausea, vomiting,
IV COMPATIBILITIES abdominal pain. Rare: Vaginal: Hyper-
Amiodarone (Cordarone), diltiaZEM sensitivity reaction.
(Cardizem), heparin, HYDROmorphone
(Dilaudid), magnesium sulfate, mid- ADVERSE EFFECTS/TOXIC
azolam (Versed), morphine, multivita- REACTIONS
mins, propofol (Diprivan). Antibiotic-associated colitis, other super-
infections (abdominal cramps, severe
INDICATIONS/ROUTES/DOSAGE watery diarrhea, fever) may occur during
Usual Dosage and several wks after clindamycin ther-
IV, IM: ADULTS, ELDERLY: 600–2,700 apy (including topical form). Blood dys-
mg/day in 2–4 divided doses. Maximum crasias (leukopenia, thrombocytopenia),
IM dose: 600 mg. CHILDREN: 20–40 nephrotoxicity (proteinuria, azotemia,
mg/kg/day in 3–4 divided doses. oliguria) occur rarely. Thrombophlebitis
Maximum: 2,700 mg/day. CHILDREN with IV administration.
YOUNGER THAN 1 MO: 5 mg/kg/dose
q6–12h. NEONATES: 15–20 mg/kg/day NURSING CONSIDERATIONS
divided q6–8h. BASELINE ASSESSMENT
PO: ADULTS, ELDERLY: 150–450 mg
q6h. Maximum: 1,800 mg/day. IN- Obtain baseline WBC. Question pt for his-
FANTS, CHILDREN, ADOLESCENTS: 8–40 tory of allergies. Avoid, if possible, con-
mg/kg/day in divided doses q6–8h. Max- current use of neuromuscular blocking
imum: 1,800 mg/day. NEONATES: 5 mg/ agents.
kg/dose q6–12 hrs. INTERVENTION/EVALUATION

Bacterial Vaginosis Monitor daily pattern of bowel activ-


Intravaginal: (Cream):  ADULTS: One ity, stool consistency. Report diarrhea
applicatorful at bedtime for 3 days in non- promptly due to potential for serious
pregnant pts or for 7 days in pregnant pts. colitis (even with topical or vaginal
(Clindesse):  ADULTS: One applicatorful ­administration). Assess skin for rash (dry-

underlined – top prescribed drug


cloBAZam 255
ness, irritation) with topical application. gag reflex, respiratory disease, sleep
With all routes of administration, be alert apnea, concomitant poor CYP2C19 me-
for superinfection: fever, vomiting, diar- tabolizers, pts at risk for falls, myasthenia
rhea, anal/genital pruritus, oral mucosal gravis, narrow-angle glaucoma. C
changes (ulceration, pain, erythema).
ACTION
PATIENT/FAMILY TEACHING
Potentiates neurotransmission of gamma-
• Continue therapy for full length of aminobutyric acid (GABA) by binding to
treatment. • Doses should be evenly GABA receptor. Depresses nerve impulse
spaced. • Take oral doses with at least transmission in motor cortex. Therapeu-
8 oz water. • Use caution when apply- tic Effect: Decreases seizure activity.
ing topical clindamycin concurrently
with peeling or abrasive acne agents, PHARMACOKINETICS
soaps, alcohol-containing cosmetics to Rapidly absorbed after PO administra-
avoid cumulative effect. • Do not apply tion. Metabolized in liver. Peak plasma
topical preparations near eyes, abraded concentration: 0.5–4 hrs. Protein bind-
areas. • Report severe persistent diar- ing: 80–90%. Primarily excreted in
rhea, cramps, bloody stool. • Vaginal: urine. Unknown if removed by dialysis.
In event of accidental contact with eyes, Half-life: 36–42 hrs.
rinse with large amounts of cool tap wa-
ter. • Do not engage in sexual inter- LIFESPAN CONSIDERATIONS
course during treatment. • Wear sani- Pregnancy/Lactation: Excreted in
tary pad to protect clothes against stains. breast milk. Hormonal contraceptives
Tampons should not be used. may have decreased effectiveness. Non-
hormonal contraception recommended.
Children: Safety and efficacy not es-
cloBAZam tablished in pts younger than 2 yrs. El-
derly: May have decreased clearance
kloe-ba-zam levels (initial dose 5 mg/day).
(Onfi, Sympazan)
Do not confuse cloBAZam with INTERACTIONS
clonazePAM or cloZAPine. DRUG: CYP2C19 inhibitors (e.g., flu-
conazole, fluvoxaMINE, omeprazole,
uCLASSIFICATION ticlopidine) may increase concentra-
PHARMACOTHERAPEUTIC: Ben- tion/effect. Alcohol, other CNS depres-
zodiazepine (Schedule IV). CLINI- sants (e.g., LORazepam, morphine,
CAL: Anticonvulsant. zolpidem) may increase CNS depres-
sion. May decrease effects of hormonal
contraceptives. CYP2C19 inducers
USES (e.g., prednisone, rifAMPin) may de-
Adjunctive treatment of seizures associated crease concentration/effect. OLANZapine
with Lennox-Gastaut syndrome in pts 2 yrs may increase adverse effects. HERBAL:
of age and older. OFF-LABEL: Catamenial Herbs with sedative properties (e.g.,
epilepsy; epilepsy (monotherapy). chamomile, kava kava, valerian) may
increase CNS depression. St. John’s wort
PRECAUTIONS may decrease effects. FOOD: None known.
Contraindications: Hypersensitivity to LAB VALUES: None significant.
cloBAZam. Cautions: Elderly, debilitated,
mild to moderate hepatic impairment, AVAILABILITY (Rx)
preexisting muscle weakness or ataxia, Suspension, Oral: 2.5 mg/mL. Tablets: 10
concomitant CNS depressants, impaired mg, 20 mg. Film, Oral: 5 mg, 10 mg, 20 mg.

Canadian trade name Non-Crushable Drug High Alert drug


256 cloBAZam

ADMINISTRATION/HANDLING appetite, dysarthria, pyrexia, dysphagia,


• May give without regard to food. • bronchitis.
Tablets may be crushed and mixed with
C ADVERSE EFFECTS/TOXIC
applesauce. • Shake suspension well.
REACTIONS
Use oral syringe supplied with suspension.
Oral Film May increase risk of suicidal behav-
• Apply on top of tongue where it can ior/ideation (less than 1%). Physi-
dissolve. Apply only one at a time. • Do cal dependence can increase with
not give with liquids; ensure swallowing higher doses or concomitant alcohol/
of a normal manner. • Pt should not drug abuse. Abrupt benzodiazepine
chew, spit, or talk as film dissolves. withdrawal may present as profuse
sweating, cramping, nausea, vomiting,
INDICATIONS/ROUTES/DOSAGE muscle pain, convulsions, psychosis,
Seizure Control (Lennox-Gastaut hallucinations, aggression, tremor,
Syndrome) anxiety, insomnia. Overdose may re-
PO: ADULTS, CHILDREN WEIGHING 30 KG sult in confusion, lethargy, diminished
OR LESS: Initially, 5 mg once daily for reflexes, respiratory depression, coma.
at least 7 days, then increase to 5 mg Antidote: Flumazenil (see Appendix J
twice for at least 7 days, then increase for dosage). Decreased mobility may
to 10 mg twice daily. Maximum: 20 potentiate higher risk of pneumonia.
mg/day. ADULTS, CHILDREN WEIGH-
NURSING CONSIDERATIONS
ING MORE THAN 30 KG: Initially, 5 mg
twice daily for at least 7 days, then in- BASELINE ASSESSMENT
crease to 10 mg twice daily for at least Offer emotional support. Review history
7 days, then increase to 20 mg twice of seizure disorder (frequency, duration,
daily. Maximum: 40 mg/day. ELDERLY intensity, level of consciousness [LOC]).
WEIGHING MORE THAN 30 KG, HEPATIC IM- Question history of alcohol use. Obtain
PAIRMENT, CYP2C19 POOR METABOLIZERS: baseline vital signs. Assess history of de-
Initially, 5 mg once daily for at least 7 pression/suicidal ideation.
days, then increase to 5 mg twice daily
for at least 7 days, then increase to 10 INTERVENTION/EVALUATION
mg twice daily. After 1 wk, may increase Monitor for excess sedation, respiratory
to 20 mg twice daily. ELDERLY WEIGHING depression, suicidal ideation. Implement
30 KG OR LESS, HEPATIC IMPAIRMENT, seizure precautions, observe frequently
CYP2C19 POOR METABOLIZERS: Initially, for seizure activity. Assist with ambulation
5 mg once daily for at least 2 wks, then if drowsiness, dizziness occurs. Evalu-
5 mg twice daily for at least 1 wk, then ate for therapeutic response. Encourage
10 mg twice daily. turning, coughing, deep breathing for
pts with decreased mobility or who are
Dosage in Renal Impairment bedridden.
No dose adjustment.
PATIENT/FAMILY TEACHING
SIDE EFFECTS • Avoid tasks that require alertness, mo-
Frequent (26%–10%): Sleepiness, URI, tor skills until response to drug is estab-
lethargy. Occasional (9%–5%): Drool- lished. • Do not abruptly discontinue
ing, nausea, vomiting, constipation, medication. • If tapering, monitor for
irritability, ataxia, insomnia, cough, drug withdrawal symptoms. • Avoid al-
fatigue. Rare (4%–2%): Psychomotor cohol. • Report depression, aggres-
hyperactivity, UTI, decreased/increased sion, thoughts of suicide/self-harm, ex-
cessive drowsiness.

underlined – top prescribed drug


clofarabine 257
vaccines (live). HERBAL: Echinacea
clofarabine may decrease effect. Herbals with hy-
pertensive properties (e.g., licorice,
kloe-far-a-bine yohimbe) or hypotensive properties C
(Clolar) (e.g., garlic, ginger, ginkgo biloba)
Do not confuse clofarabine with may alter effects. FOOD: None known.
cladribine or clevidipine. LAB VALUES: May increase serum creati-
nine, uric acid, ALT, AST, bilirubin.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Anti- AVAILABILITY (Rx)
metabolite (purine analog). CLINI- Injection, Solution: 1 mg/mL (20-mL vial).
CAL: Antineoplastic.
ADMINISTRATION/HANDLING
USES IV
Treatment of pediatric pts (1–21 yrs) with Reconstitution • Filter clofarabine
relapsed or refractory acute lymphoblastic through sterile, 0.2-micrometer syringe
leukemia (ALL). OFF-LABEL: Acute myeloid filter prior to dilution with D5W or 0.9%
leukemia (AML) in adults 60 yrs or older. NaCl to final concentration of 0.15–0.4
Treatment of relapsed/refractory ALL. mg/mL.
Rate of administration • Administer
PRECAUTIONS
over 1–2 hrs. • Continuously infuse IV
Contraindications: Hypersensitivity to clofar- fluids to decrease risk of tumor lysis
abine. Cautions: Dehydration, hypotension, syndrome, other adverse events.
concomitant nephrotoxic or hepatotoxic Storage • Store undiluted or diluted
medications, renal/hepatic impairment. solution at room temperature. • Use
ACTION diluted solution within 24 hrs.
Metabolized intracellularly to clofara- IV INCOMPATIBILITIES
bine triphosphate. Inhibits ribonucleo- Do not administer any other medication
side reductase, which inhibits DNA through same IV line.
synthesis. Competes with DNA polymers,
decreasing cell replication. Therapeu- INDICATIONS/ROUTES/DOSAGE
tic Effect: Decreases cell replication, Acute Lymphoblastic Leukemia (ALL)
inhibits cell repair. Produces cell death. IV: CHILDREN 1–21 YRS: 52 mg/m2 over
PHARMACOKINETICS 2 hrs once daily for 5 consecutive days;
repeat q2–6wks following recovery or
Protein binding: 47%. Metabolized intracel-
return to baseline organ function. (Sub-
lularly. Primarily excreted in urine (40%–
sequent cycles should begin no sooner
60% unchanged). Half-life: 5.2 hrs.
than 14 days from day 1 of previous
LIFESPAN CONSIDERATIONS cycle and when ANC is 750 cells/mm3
or greater.)
Pregnancy/Lactation: May cause
fetal harm. Breastfeeding not recom- Dosage in Renal Impairment
mended. Children: Safety and efficacy Dosage is modified based on creatinine
not established in pts younger than 1 yr. El- clearance.
derly: No age-related precautions noted.
Creatinine
INTERACTIONS Clearance Dosage
DRUG: May decrease therapeutic ef- 30–60 mL/min Decrease dose
fect of BCG (intravesical), vaccines by 50%
(live). May increase adverse effects of Less than 30 mL/min Use with caution

Canadian trade name Non-Crushable Drug High Alert drug


258 clomiPRAMINE
Dosage in Hepatic Impairment PATIENT/FAMILY TEACHING
Baseline impairment: No dose adjust- • Do not have immunizations without
ment. Hepatotoxicity during treat- physician’s approval (drug lowers resis-
C ment; Grade 3 or higher increase in tance). • Avoid contact with anyone who
bilirubin: Discontinue. May restart at recently received a live virus vac-
25% dose reduction following recovery cine. • Avoid crowds, those with infec-
to baseline. tion. • Avoid pregnancy; pts of child-
bearing potential should use effective
SIDE EFFECTS contraception. • Maintain strict oral hy-
Frequent (83%–20%): Vomiting, nausea, giene and frequent handwashing. • Re-
diarrhea, pruritus, headache, fever, der- port fever, respiratory distress, prolonged
matitis, rigors, abdominal pain, fatigue, nausea, vomiting, diarrhea, easy bruising.
tachycardia, epistaxis, anorexia, pete-
chiae, limb pain, hypotension, anxiety,
constipation, edema. Occasional (19%–
11%): Cough, mucosal inflammation,
clomiPRAMINE
erythema, flushing, hematuria, dizziness, kloe-mip-rah-meen
gingival bleeding, injection site pain, (Anafranil, Apo-ClomiPRAMINE ,
respiratory distress, pharyngitis, back Novo-ClomiPRAMINE )
pain, palmar-plantar erythrodysesthesia
syndrome, myalgia, oral candidiasis,
j BLACK BOX ALERT jIncreased
risk of suicidal ideation and behav-
hypertension, depression, irritability, ar- ior in children, adolescents, young
thralgia, anorexia. Rare (10%): Tremor, adults 18–24 yrs with major depres-
weight gain, drowsiness. sive disorder, other psychiatric
disorders.
ADVERSE EFFECTS/TOXIC Do not confuse Anafranil with
REACTIONS enalapril, or clomiPRAMINE with
Neutropenia occurred in 57% of pts; chlorproMAZINE, clevidipine,
pericardial effusion in 35%; left ven- clomiPHENE, or desipramine.
tricular systolic dysfunction in 27%;
uCLASSIFICATION
hepatomegaly, jaundice in 15%; pleural
effusion, pneumonia, bacteremia in 10%; PHARMACOTHERAPEUTIC: Tricyclic.
capillary leak syndrome in less than 10%. CLINICAL: Antidepressant.

NURSING CONSIDERATIONS USES


BASELINE ASSESSMENT Treatment of obsessive-compulsive disor-
Question possibility of pregnancy. Obtain der. OFF-LABEL: Depression, panic attacks.
CBC, BMP, LFT, CrCl prior to therapy. PRECAUTIONS
INTERVENTION/EVALUATION Contraindications: Hypersensitivity to clo-
Monitor CBC, renal function test, LFT, se- miPRAMINE, other tricyclic agents. Acute
rum uric acid. Monitor respiratory status, recovery period after MI, use of MAOIs in-
cardiac function. Monitor daily pattern tended for psychiatric disorders (concur-
of bowel activity, stool consistency. As- rently or within 14 days of discontinuing
sess for GI disturbances. Assess skin for either clomipramine or MAOI). Initiation
pruritus, dermatitis, petechiae, erythema in pts receiving linezolid or methylene
on palms of hands and soles of feet. As- blue. Cautions: Pts at high risk for sui-
sess for fever, sore throat; obtain blood cide, prostatic hypertrophy, history of
cultures to detect evidence of infection. urinary retention/obstruction, narrow-
Ensure adequate hydration. angle glaucoma, seizures, cardiovascular/
hepatic/renal disease, hyperthyroidism,
underlined – top prescribed drug
clomiPRAMINE 259
alcoholism, xerostomia, visual problems, or hypotensive properties (e.g., gar-
elderly, constipation, history of bowel ob- lic, ginger, ginkgo biloba) may alter
struction. Tumors of the adrenal medulla effects. FOOD: Grapefruit products
(e.g., pheochromocytoma). may increase concentration, toxicity. LAB C
VALUES: May alter serum glucose, ECG
ACTION readings.
Blocks reuptake of neurotransmitters
(norepinephrine, serotonin) at CNS pre- AVAILABILITY (Rx)
synaptic membranes, increasing avail- Capsules: 25 mg, 50 mg, 75 mg.
ability at postsynaptic receptor sites.
Therapeutic Effect: Reduces obses- ADMINISTRATION/HANDLING
sive-compulsive behavior. PO
• May give with food to decrease risk of
PHARMACOKINETICS GI disturbance. • Recommend bedtime
Rapidly absorbed. Metabolized in liver. administration.
Eliminated in urine (51%–60%), feces
(24%–32%). Half-life: 20–30 hrs. INDICATIONS/ROUTES/DOSAGE
Note: Following dose titration, may give
LIFESPAN CONSIDERATIONS once-daily dose at bedtime.
Pregnancy/Lactation: Distributed in
breast milk. Children: Increased risk Obsessive-Compulsive Disorder (OCD)
of suicidal ideation, behavior noted in PO: ADULTS, ELDERLY: Initially, 25mg/day.
children, adolescents. Safety and effec- May gradually increase to 100 mg/day in
tiveness in pts younger than 10 yrs not divided doses in the first 2 wks. Mainte-
established. Elderly: Not recommended nance: After initial titration, wait 2–3 wks
in elderly due to anticholinergic effects, between dosing. May further increase
potential for sedation, orthostatic hypo- up to 250 mg/day at bedtime. Maxi-
tension. mum: 250 mg/day. CHILDREN 10 YRS AND
OLDER: Initially, 25 mg/day. May gradually
INTERACTIONS increase up to maximum of 3 mg/kg/day
DRUG: Alcohol, other CNS depres- or 100 mg in divided doses (whichever is
sants (e.g., lorazepam, morphine, lowest). Maintenance: After initial titra-
zolpidem) may increase CNS, respi- tion, wait 2–3 wks between dosing. May
ratory depression, hypotensive effect. further increase to 3 mg/kg or 200 mg/
CNS depressants (e.g., alcohol, day at bedtime (whichever is less).
morphine, oxyCODONE, zolpidem)
Dosage in Renal/Hepatic Impairment
may increase CNS depression. Strong
CYP2C19, CYP2D6 inhibitors (e.g., Use caution.
buPROPion, FLUoxetine, paroxetine) SIDE EFFECTS
may increase concentration/effect. May
enhance arrhythmogenic effect of drone- Frequent (30%–15%): Ejaculatory failure,
darone. Linezolid, MAOIs (e.g., dry mouth, somnolence, tremors, diz-
selegiline, phenelzine) may increase ziness, headache, constipation, fatigue,
serotonergic effect. Anticholinergics nausea. Occasional (14%–5%): Impotence,
(e.g., aclidinium, ipratropium, ume- diaphoresis, dyspepsia, sexual dysfunction,
clidinium) may increase anticholinergic dysmenorrhea, nervousness, weight gain,
effect. HERBAL: Gota kola, kava kava, pharyngitis. Rare (less than 5%): Diarrhea,
valerian may increase CNS depression. myalgia, rhinitis, increased appetite, pares-
St. John’s wort may decrease concentra- thesia, memory impairment, anxiety, rash,
tion/effect. Herbals with hypertensive pruritus, anorexia, abdominal pain, vom-
properties (e.g., licorice, yohimbe) iting, flatulence, flushing, UTI, back pain.

Canadian trade name Non-Crushable Drug High Alert drug


260 clonazePAM

ADVERSE EFFECTS/TOXIC uCLASSIFICATION


REACTIONS PHARMACOTHERAPEUTIC: Ben-
Overdose may produce seizures, cardio- zodiazepine (Schedule IV). CLINI-
C vascular effects (severe orthostatic hypo- CAL: Anticonvulsant, antianxiety.
tension, dizziness, tachycardia, palpita-
tions, arrhythmias), altered tem­perature
regulation (hyperpyrexia, hyp­othermia). USES
Abrupt discontinuation after prolonged Adjunct in treatment of Lennox-Gastaut
therapy may produce headache, malaise, syndrome (petit mal variant epilepsy);
nausea, vomiting, vivid dreams. Anemia, akinetic, myoclonic seizures; absence sei-
agranulocytosis have been noted. zures (petit mal) unresponsive to succin-
imides. Treatment of panic disorder. OFF-
NURSING CONSIDERATIONS LABEL: Burning mouth syndrome, REM
BASELINE ASSESSMENT
sleep behavior disorder, essential tremor.
Assess psychological status, thought con- PRECAUTIONS
tent, level of interest, mood, behavior, Contraindications: Hypersensitivity
suicidal ideation. to clonazePAM. Active narrow-angle
INTERVENTION/EVALUATION glaucoma, severe hepatic disease. Cau-
Supervise suicidal-risk pt closely during tions: Renal/hepatic impairment, im-
early therapy (as depression lessens, en- paired gag reflex, chronic respiratory dis-
ergy level improves, increasing suicide ease, elderly, debilitated pts, depression,
potential). Assess appearance, behavior, pts at risk of suicide or drug dependence,
speech pattern, level of interest, mood. concomitant use of other CNS depressants.
PATIENT/FAMILY TEACHING ACTION
• May cause dry mouth, constipation, Enhances activity of GABA; depresses
blurred vision. Avoid tasks that require alert- nerve impulse transmission in motor
ness, motor skills until response to drug is cortex. Therapeutic Effect: Produces
established. • Tolerance to postural hypo- anxiolytic, anticonvulsant effects.
tension, sedative, anticholinergic effects usu-
ally develop during early therapy. • Maxi- PHARMACOKINETICS
mum therapeutic effect may be noted in 2–4 Route Onset Peak Duration
wks. • Do not abruptly discontinue medi- PO 20–60 — 12 hrs or
cation. • Daily dose may be given at bed- min less
time to minimize daytime sedation. • Avoid
alcohol. • Report worsening depression, Well absorbed from GI tract. Protein
suicidal ideation, change in behavior. binding: 85%. Metabolized in liver. Ex-
creted in urine. Not removed by hemodi-
alysis. Half-life: 18–50 hrs.
clonazePAM LIFESPAN CONSIDERATIONS
kloe-naz-e-pam Pregnancy/Lactation: Crosses placenta.
(KlonoPIN, Rivotril ) May be distributed in breast milk. Chronic
ingestion during pregnancy may produce
j BLACK BOX ALERT jConcomi- withdrawal symptoms, CNS depression in
tant use with opioids may result
in profound sedation, respiratory neonates. Children: Long-term use may
depression, coma, and death. adversely affect physical/mental develop-
Do not confuse clonazePAM or ment. Elderly: Not recommended in el-
KlonoPIN with cloBAZam, cloNI- derly due to anticholinergic effects, potential
Dine, cloZAPine, or LORazepam. for sedation, orthostatic hypotension.

underlined – top prescribed drug


clonazePAM 261

INTERACTIONS Panic Disorder


DRUG: Alcohol, other CNS depres- PO: ADULTS, ELDERLY: Initially, 0.25 mg
sants (e.g., lorazepam, morphine, twice daily. Increase in increments of
zolpidem) may increase CNS depressant 0.125–0.25 mg twice daily every 3 days. C
effect. Strong CYP3A4 inhibitors (e.g., Target dose: 1 mg/day. Maximum: 4
clarithromycin, ketoconazole, rito- mg/day. Note: Discontinue gradually by
navir) may increase concentration/effect. 0.125 mg twice daily q3days until com-
Strong CYP3A4 inducers (e.g., carBAM- pletely withdrawn.
azepine, phenytoin, rifAMPin) may de- Dosage in Renal Impairment
crease concentration/effect. HERBAL: Herbs Use caution.
with sedative properties (e.g., chamo-
mile, kava kava, valerian) may increase Dosage in Hepatic Impairment
CNS depression. St. John’s wort may de- Mild to moderate impairment: Use
crease concentration/effects. FOOD: None with caution. Severe impairment: Con-
known. LAB VALUES: None significant. traindicated.

AVAILABILITY (Rx) SIDE EFFECTS


Tablets: (Klonopin): 0.5 mg, 1 mg, 2 mg. Frequent (37%–11%): Mild, transient
Tablets (Orally Disintegrating): 0.125 mg, drowsiness; ataxia, behavioral distur-
0.25 mg, 0.5 mg, 1 mg, 2 mg. bances (aggression, irritability, agita-
tion), esp. in children. Occasional (10%–
ADMINISTRATION/HANDLING 5%): Dizziness, ataxia, URI, fatigue. Rare
PO (4% or less): Impaired memory, dysar-
• Give without regard to food. • Swal- thria, nervousness, sinusitis, rhinitis,
low whole with water. constipation, allergic reaction.

Orally Disintegrating Tablet ADVERSE EFFECTS/TOXIC


• Open pouch, peel back foil; do not REACTIONS
push tablet through foil. • Remove tablet Abrupt withdrawal may result in pro-
with dry hands, place in mouth. • Swal- nounced restlessness, irritability, insomnia,
low with or without water. • Use immedi- hand tremors, abdominal/muscle cramps,
ately after removing from package. diaphoresis, vomiting, status epilepticus.
Overdose results in drowsiness, confusion,
INDICATIONS/ROUTES/DOSAGE diminished reflexes, coma. Antidote: Flu-
Seizures mazenil (see Appendix J for dosage).
PO: ADULTS, ELDERLY, CHILDREN 10 YRS AND
OLDER: Initial dose not to exceed 1.5 mg/ NURSING CONSIDERATIONS
day in 3 divided doses; may be increased in BASELINE ASSESSMENT
0.5- to 1-mg increments every 3 days until
Review history of seizure disorder (fre-
seizures are controlled or adverse effects
quency, duration, intensity, level of con-
occur. Maintenance: 2–8 mg/day in 1–2
sciousness [LOC]). For panic attack,
divided doses. Maximum: 20 mg/day.
assess motor responses (agitation, trem-
INFANTS, CHILDREN YOUNGER THAN 10 YRS
bling, tension), autonomic responses
OR WEIGHING LESS THAN 30 KG: 0.01–0.03
(cold/clammy hands, diaphoresis).
mg/kg/day (maximum initial dose: 0.05
mg/kg/day) in 2–3 divided doses; may be INTERVENTION/EVALUATION
increased by no more than 0.25–0.5 mg Observe for excess sedation, respiratory
every 3 days until seizures are controlled or depression, suicidal ideation. Assess chil-
adverse effects occur. Maintenance: 0.1– dren, elderly for paradoxical reaction,
0.2 mg/kg/day in 3 divided doses. Maxi- particularly during early therapy. Initiate
mum: 0.2 mg/kg/day. seizure precautions, observe frequently for
Canadian trade name Non-Crushable Drug High Alert drug
262 cloNIDine
recurrence of seizure activity. Assist with headaches, treatment of diarrhea in
ambulation if drowsiness, ataxia occur. For diabetes mellitus, treatment of dysmen-
pts on long-term therapy, CBC, BMP, LFT orrhea, menopausal flushing, alcohol de-
C should be performed periodically. Evaluate pendence, glaucoma, cloZAPine-induced
for therapeutic response: decreased inten- sialorrhea, Tourette’s syndrome, insom-
sity and frequency of seizures or, if used nia in children.
in panic attack, calm facial expression,
decreased restlessness. PRECAUTIONS
Contraindications: Hypersensitivity to
PATIENT/FAMILY TEACHING
cloNIDine. Epidural: Contraindicated
• Avoid tasks that require alertness, motor in pts with bleeding diathesis or infection
skills until response to drug is estab- at the injection site; pts receiving antico-
lished. • Do not abruptly discontinue agulation therapy. Cautions: Depression,
medication after long-term therapy. • Strict elderly. Severe coronary insufficiency, re-
maintenance of drug therapy is essential for cent MI, cerebrovascular disease, chronic
seizure control. • Avoid alcohol. • Re- renal impairment, preexisting bradycar-
port depression, thoughts of suicide/self- dia, sinus node dysfunction, conduction
harm, excessive drowsiness, GI symptoms, disturbances; concurrent use with di-
worsening or loss of seizure control. goxin, diltiaZEM, metoprolol, verapamil.
ACTION
cloNIDine Stimulates alpha2-adrenergic receptors in
the brainstem, reducing sympathetic out-
klon-i-deen flow from the CNS. Epidural: Prevents pain
(Catapres, Catapres-TTS, Dixarit , signal transmission to brain and produces
Duraclon, Kapvay) analgesia at pre- and post-alpha-adrenergic
j BLACK BOX ALERT jEpidural: receptors in spinal cord. ADHD: Mecha-
Not to be used for perioperative, nism of action unknown. Therapeutic
obstetric, or postpartum pain. Must
dilute concentrated epidural inject- Effect: Reduces peripheral resistance; de-
able (500 mcg/mL) prior to use. creases B/P, heart rate. Produces analgesia.
Do not confuse Catapres with
Cataflam, or cloNIDine with PHARMACOKINETICS
clomiPHENE, clonazepam, Route Onset Peak Duration
KlonoPIN, or quiNIDine. PO 0.5–1 hr 2–4 hrs 6–10 hrs

uCLASSIFICATION Well absorbed from GI tract. Transder-


PHARMACOTHERAPEUTIC: Alpha 2- mal best absorbed from chest and upper
adrenergic agonist. CLINICAL: Anti- arm; least absorbed from thigh. Protein
hypertensive. binding: 20%–40%. Metabolized in liver.
Primarily excreted in urine. Minimally re-
moved by hemodialysis. Half-life: 6–20
USES hrs (increased in renal impairment).
Immediate-Release, Transdermal LIFESPAN CONSIDERATIONS
Patch: Treatment of hypertension alone
or in combination with other antihyper- Pregnancy/Lactation: Crosses pla-
tensive agents. Kapvay: Treatment of centa. Distributed in breast milk. Chil-
dren: More sensitive to effects; use
attention-deficit hyperactivity disorder
(ADHD). Epidural: (Additional) Com- caution. Elderly: Not recommended in
bined with opiates for relief of severe elderly due to high risk of CNS adverse
cancer pain. OFF-LABEL: Opioid or nico- effects, orthostatic hypotension. Avoid as
tine withdrawal, prevention of migraine first-line antihypertensive.

underlined – top prescribed drug


cloNIDine 263

INTERACTIONS IV INCOMPATIBILITIES
DRUG: CNS depressants (e.g., alcohol, None known.
morphine, oxyCODONE, zolpidem)
may increase CNS depression. May increase IV COMPATIBILITIES C
AV blocking effect of beta blockers (e.g., Bupivacaine (Marcaine, Sensorcaine),
atenolol, carvedilol, metoprolol). Tri- fentaNYL (Sublimaze), heparin, ketamine
cyclic antidepressants (e.g., amitrip- (Ketalar), lidocaine, LORazepam (Ativan).
tyline, doxepin, nortriptyline) may de-
crease effect (may require increased dose of INDICATIONS/ROUTES/DOSAGE
cloNIDine). Digoxin, diltiaZEM, meto- Hypertension
prolol, verapamil may increase risk of PO: ADULTS: (Immediate-Release):
serious bradycardia. HERBAL: Herbs with Initially, 0.1 mg twice a day. Increase by 0.1
sedative properties (e.g., chamomile, mg/day at wkly intervals. Dosage range:
kava kava, valerian) may increase CNS 0.1–0.8 mg/day in 2 divided doses.
depression. Herbals with hypertensive Maximum: 2.4 mg/day. Usual dose
properties (e.g., licorice, yohimbe) or range: 0.1–0.2 mg twice daily. EL-
hypotensive properties (e.g., garlic, DERLY: Initially, 0.1 mg at bedtime. May
ginger, ginkgo biloba) may alter effects. increase gradually. CHILDREN 12 YRS AND
FOOD: None known. LAB VALUES: None OLDER: Initially, 0.2 mg/day in 2 divided
significant. doses. May increase gradually at 7-day
intervals in 0.1 mg/day increments. Maxi-
AVAILABILITY (Rx) mum: 2.4 mg/day.
Injection Solution: (Duraclon): 100 mcg/ Transdermal: ADULTS, ELDERLY: Ini-
mL, 500 mcg/mL. Tablets: (Catapres): 0.1 tially, system delivering 0.1 mg/24 hrs ap-
mg, 0.2 mg, 0.3 mg. Transdermal Patch: plied once q7days. May increase by 0.1
(Catapres-TTS): 2.5 mg (release at 0.1 mg at 1- to 2-wk intervals. Usual dosage
mg/24 hrs), 5 mg (release at 0.2 mg/24 range: 0.1–0.3 mg once wkly.
hrs), 7.5 mg (release at 0.3 mg/24 hrs).
Acute Hypertension
Extended-Release Tablets: (Kapvay): PO: ADULTS: Initially, 0.1–0.2 mg fol-
0.1 mg. lowed by 0.1 mg every hr if necessary, up
to maximum total dose of 0.7 mg.
ADMINISTRATION/HANDLING
PO Attention-Deficit Hyperactivity Disorder
• Give without regard to food. • Tab- (ADHD)
lets may be crushed. • Give last oral Note: When discontinuing, taper gradu-
dose just before bedtime. • Swallow ally over 1–2 wks. (Extended-Release Tab-
extended-release tablets whole; do not lets): Taper by 0.1 mg or less q3–7 days.
break, crush, dissolve, or divide. PO: CHILDREN WEIGHING 45 KG OR
LESS: (Immediate-Release): Initially 0.05
Transdermal mg/day at bedtime. May increase in incre-
• Apply transdermal system to dry, hair- ments of 0.05 mg/day q3–7days up to 0.2
less area of intact skin on upper arm or mg/day (27–40.5 kg), 0.3 mg/day (40.5–
chest. • Rotate sites (prevents skin ir- 45 kg). MORE THAN 45 KG: (Immediate Re-
ritation). • Do not trim patch to adjust lease): 0.1 mg at bedtime. May increase
dose. 0.1 mg/day q3–7 days. Maximum: 0.4
mg/day. Extended-Release Tablet (Kap-
Epidural vay):  CHILDREN 6 YRS AND OLDER: Initially,
• Must be administered only by medical 0.1 mg daily at bedtime. May increase in
personnel trained in epidural manage- increments of 0.1 mg/day at wkly intervals
ment. (Maximum: 0.4 mg/day). Doses should

Canadian trade name Non-Crushable Drug High Alert drug


264 clopidogrel
be taken twice daily with higher split dose PATIENT/FAMILY TEACHING
given at ­bedtime. • Sugarless gum, sips of water may re-
lieve dry mouth. • Avoid tasks that re-
C Severe Pain quire alertness, motor skills until response
Epidural: ADULTS, ELDERLY: 30–40 mcg/ to drug is established. • To reduce hypo-
hr. CHILDREN: Range: 0.5–2 mcg/kg/hr, not tensive effect, rise slowly from lying to
to exceed adult dose. standing. • Skipping doses or voluntarily
Dosage in Renal/Hepatic Impairment
discontinuing drug may produce severe
No dose adjustment. rebound hypertension. • Avoid alco-
hol. • If patch loosens during 7-day ap-
SIDE EFFECTS plication period, secure with adhesive
cover.
Frequent (40%–10%): Dry mouth, drowsi-
ness, dizziness, sedation, constipation. Oc-
casional (5%–1%): Tablets, Injection: De-
pression, pedal edema, loss of appetite,
decreased sexual function, itching eyes,
clopidogrel
dizziness, nausea, vomiting, nervousness. kloe-pid-oh-grel
Transdermal: Pruritus, redness or dark- (Plavix)
ening of skin. Rare (less than 1%): Night-
mares, vivid dreams, feeling of coldness in
j BLACK BOX ALERT jDiminished
effectiveness in CYP2C19 metaboliz-
distal extremities (esp. the digits). ers increases risk for cardiovascular
events. Pts with CYP2C19*2 and/
ADVERSE EFFECTS/TOXIC or CYP2C19*3 alleles may have
reduced platelet inhibition.
REACTIONS Do not confuse Plavix with
Overdose produces profound hypoten- Elavil or Paxil.
sion, irritability, bradycardia, respiratory
depression, hypothermia, miosis (pupil- uCLASSIFICATION
lary constriction), arrhythmias, apnea. PHARMACOTHERAPEUTIC: Thieno-
Abrupt withdrawal may result in rebound pyridine derivative. CLINICAL: Anti-
hypertension associated with nervous- platelet.
ness, agitation, anxiety, insomnia, pares-
thesia, tremor, flushing, diaphoresis. May
produce sedation in pts with acute CVA. USES
To reduce rate of MI and stroke (with
NURSING CONSIDERATIONS aspirin) in pts with non–ST-segment el-
BASELINE ASSESSMENT evation acute coronary syndrome (ACS),
Obtain B/P immediately before each dose acute ST-elevation MI (STEMI); pts with
is administered, in addition to regular history of recent MI or stroke, or estab-
monitoring (be alert to B/P fluctuations). lished peripheral arterial disease (PAD).
OFF-LABEL: Graft patency (saphenous
INTERVENTION/EVALUATION vein), stable coronary artery disease (in
Monitor B/P, pulse, mental status. Monitor combination with aspirin). Initial treat-
daily pattern of bowel activity, stool con- ment of ACS in pts allergic to aspirin.
sistency. If cloNIDine is to be withdrawn,
discontinue concurrent beta-blocker PRECAUTIONS
therapy several days before discontinu- Contraindications: Hypersensitivity to
ing cloNIDine (prevents cloNIDine with- clopidogrel. Active bleeding (e.g., peptic
drawal hypertensive crisis). Slowly reduce ulcer, intracranial hemorrhage). Cautions:
cloNIDine dosage over 2–4 days. Severe hepatic/renal impairment, pts at risk

underlined – top prescribed drug


clopidogrel 265
of increased bleeding (e.g., trauma), con- ADMINISTRATION/HANDLING
current use of anticoagulants. Avoid con- PO
current use of CYP2C19 inhibitors (e.g., • Give without regard to food. • Avoid
omeprazole). grapefruit products. C
ACTION INDICATIONS/ROUTES/DOSAGE
Active metabolite irreversibly blocks Recent MI, Stroke, PAD
P2Y12 component of ADP receptors on PO: ADULTS, ELDERLY: 75 mg once daily.
platelet surface, preventing activation of
GPIIb/IIIa receptor complex. Thera- Acute Coronary Syndrome (ACS), Unstable
peutic Effect: Inhibits platelet aggre- Angina/NSTEMI
gation. PO: ADULTS, ELDERLY: Initially, loading
dose of 300–600 mg, then 75 mg once
PHARMACOKINETICS daily (in combination with aspirin for up
Route Onset Peak Duration to 12 months, then aspirin indefinitely).
PO 2 hrs 5–7 days (with 5 days af-
repeated ter last ACS (STEMI)
doses of 75 dose Note: Continue for at least 14 days up to
mg/day) 12 mos in absence of bleeding.
PO: ADULTS, ELDERLY 75 YRS OR
Rapidly absorbed. Protein binding: YOUNGER: Initially 300-mg loading dose,
98%. Metabolized in liver. Eliminated then 75 mg once daily. ELDERLY OLDER
equally in the urine and feces. Half-life: THAN 75 YRS: 75 mg once daily.
8 hrs.
ACS (PCI)
LIFESPAN CONSIDERATIONS PO: ADULTS, ELDERLY: Initially, 600 mg,
Pregnancy/Lactation: Unknown if then 75 mg once daily (in combination
drug crosses placenta or is distributed with aspirin) for at least 12 months.
in breast milk. Children: Safety and ef-
ficacy not established. Elderly: No age- Dosage in Renal Impairment
related precautions noted. No dose adjustment.

INTERACTIONS Dosage in Hepatic Impairment


DRUG: May increase adverse effects of Use caution.
apixaban, dabigatran, edoxaban, SIDE EFFECTS
warfarin. Strong CYP2C19 inhibi-
tors (e.g., fluvoxaMINE, FLUoxetine) Frequent (15%): Skin disorders. Occa-
may decrease concentration/effect. sional (8%–6%): Upper respiratory tract
HERBAL: Herbals with anticoagu- infection, chest pain, flu-like symptoms,
lant/antiplatelet properties (e.g., headache, dizziness, arthralgia. Rare
garlic, ginger, ginkgo biloba), glu- (5%–3%): Fatigue, edema, hypertension,
cosamine may increase risk of bleed- abdominal pain, dyspepsia, diarrhea,
ing. FOOD: Grapefruit products may nausea, epistaxis, dyspnea, rhinitis.
decrease effects. LAB VALUES: May in- ADVERSE EFFECTS/TOXIC
crease serum bilirubin, ALT, AST, choles- REACTIONS
terol, uric acid. May decrease neutrophil
count, platelet count. Agranulocytosis, aplastic anemia/pancy-
topenia, thrombotic thrombocytopenic
AVAILABILITY (Rx) purpura (TTP) occur rarely. Hepatitis,
Tablets: 75 mg, 300 mg. hypersensitivity reaction, anaphylactoid
reaction have been reported.

Canadian trade name Non-Crushable Drug High Alert drug


266 cloZAPine

NURSING CONSIDERATIONS USES


Management of severely ill schizophrenic
BASELINE ASSESSMENT pts who have failed to respond to other
C Obtain baseline chemistries, platelet antipsychotic therapy. Treatment of
count, PFA. Perform platelet counts be- recurrent suicidal behavior in schizo-
fore drug therapy, q2days during first phrenia or schizoaffective disorder. OFF-
wk of treatment, and wkly thereafter LABEL: Schizoaffective disorder, bipolar
until therapeutic maintenance dose is disorder, childhood psychosis, obsessive-
reached. Abrupt discontinuation of drug compulsive disorder, agitation related to
therapy produces elevated platelet count Alzheimer’s dementia.
within 5 days.
PRECAUTIONS
INTERVENTION/EVALUATION
Contraindications: Hypersensitivity to
Monitor platelet count for evidence of cloZAPine. History of cloZAPine-induced
thrombocytopenia. Assess Hgb, Hct, for agranulocytosis or severe granulocytope-
evidence of bleeding; serum ALT, AST, bil- nia. Cautions: History of seizures, cardio-
irubin, BUN, creatinine; signs/symptoms vascular disease, myocarditis, respiratory/
of hepatic insufficiency during therapy. hepatic/renal impairment, alcohol with-
PATIENT/FAMILY TEACHING drawal, high risk of suicide, paralytic ileus,
• It may take longer to stop bleeding myasthenia gravis, pts at risk for aspiration
during drug therapy. • Report any un- pneumonia, urinary retention, narrow-
usual bleeding. • Inform physicians, angle glaucoma, prostatic hypertrophy,
dentists if clopidogrel is being taken, esp. xerostomia, visual disturbances, constipa-
before surgery is scheduled or before tion, history of bowel obstruction, diabetes
taking any new drug. mellitus. History of long QT prolongation/
ventricular arrhythmias; concomitant use
of medications that prolong QT interval;
hypokalemia, hypomagnesemia.
cloZAPine ACTION
kloe-za-peen Interferes with binding of DOPamine and
(Clozaril, FazaClo, Versacloz) serotonin receptor sites. Therapeutic Ef-
fect: Diminishes schizophrenic behavior.
j BLACK BOX ALERT j
Significant risk of life-threatening
agranulocytosis, increased risk PHARMACOKINETICS
of potentially fatal cardiovascular Readily absorbed from GI tract. Protein
events, particularly myocarditis, in binding: 97%. Metabolized in liver. Ex-
elderly pts with dementia-related creted in urine. Half-life: 12 hrs.
psychosis. May cause severe or-
thostatic hypotension, bradycardia,
syncope, cardiac arrest, dose- LIFESPAN CONSIDERATIONS
dependent seizures. Pregnancy/Lactation: Crosses pla-
Do not confuse cloZAPine with centa. Avoid use during pregnancy. Dis-
clonazePAM, cloNIDine, or Klo- tributed in breast milk. Breastfeeding not
noPIN, or Clozaril with Clinoril recommended. Children: Not recom-
or Colazal. mended for use. Elderly: Avoid use in
pts with dementia.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Second- INTERACTIONS
generation (atypical) antipsychotic. DRUG: CNS depressants (e.g., alco-
CLINICAL: Antipsychotic. hol, morphine, oxyCODONE, zol-
pidem) may increase CNS depression.
underlined – top prescribed drug
cloZAPine 267
Anticholinergics (e.g., aclidinium, PO: ADULTS: Initially, 12.5 mg once
ipratropium, umeclidinium) may or twice daily. May increase by 25–50
increase anticholinergic effect. Strong mg/day over 2 wks until target dose of
CYP3A4 inhibitors (e.g., clarithro- 300–450 mg/day is achieved. May fur- C
mycin, ketoconazole, ritonavir) may ther increase by 50–100 mg/day no more
increase concentration/effect. Strong than once or twice wkly. Range: 200–600
CYP3A4 inducers (e.g., carBAM- mg/day. Maximum: 900 mg/day. EL-
azepine, phenytoin, rifAMPin) may DERLY: Initially, 12.5 mg/day for 3 days,
decrease concentration/effect. Metoclo- then 25 mg/day for 3 days. May further
pramide may increase adverse effects. increase in increments of 12.5–25 mg
HERBAL: St. John’s wort may decrease daily q3days. Mean dose: 300 mg/day.
concentration/effect. Herbals with hy- Maximum: 700 mg/day.
potensive properties (e.g., garlic,
ginger, ginkgo biloba) may alter ef- Suicidal Behavior in Schizophrenia or
fects. Herbals with sedative proper- Schizoaffective Disorder
ties (e.g., chamomile, kava kava, PO: ADULTS: Initially, 12.5 mg 1–2
valerian) may increase CNS depression. times/day. May increase in increments of
FOOD: None known. LAB VALUES: May 25–50 mg/day to a target dose of 300–450
increase serum glucose, cholesterol mg/day after 2 wks. Mean dose: 300
(rare), triglycerides (rare). mg/day. Maximum: 900 mg/day.
AVAILABILITY (Rx) Dose Modification
Suspension, Oral: (Versacloz): 50 mg/mL Leukopenia/granulocytopenia: Mild:
(100 mL). Tablets: (Clozaril): 25 mg, 50 (WBC 3,000–3,500 cells/mm3 and/or
mg, 100 mg, 200 mg. Tablets: (Orally Dis- ANC 1,500–2,000 cells/mm3): Con-
integrating [FazaClo]): 12.5 mg, 25 mg, tinue treatment, monitor WBC and
100 mg, 150 mg, 200 mg. ANC twice wkly until WBC greater than
3,500 cells/mm3 and ANC greater than
ADMINISTRATION/HANDLING 2,000 cells/mm3. Moderate: (WBC
PO 2,000–3,000 cells/mm3 and/or ANC
• Give without regard to food. • Sus- greater than 1,000 cells/mm3–1,500
pension: Use oral syringes (provided). cells/mm3): Interrupt therapy, moni-
Shake well, administer dose immediately tor WBC and ANC daily until WBC greater
after preparing. Suspension stable for than 3,000 cells/mm3 and ANC greater
100 days after initial bottle opening. than 1,500 cells/mm3, then twice wkly
until WBC greater than 3,500 cells/mm3
Orally Disintegrating Tablets and ANC greater than 2,000 cells/mm3.
• Remove from foil blister; do not push Severe: (WBC less than 2,000 cells/
tablet through foil. • Remove tablet mm3 and/or ANC less than 1,500
with dry hands, place in mouth. • Allow cells/mm3): Discontinue treatment.
to dissolve in mouth; swallow with sa- Discontinue: QTC interval greater than
liva. • If dose requires splitting tablet, 500 msec, cardiomyopathy/myocarditis,
discard unused portion. hepatotoxicity, or neuroleptic malignant
INDICATIONS/ROUTES/DOSAGE syndrome.
Schizophrenic Disorders Dosage in Renal/Hepatic Impairment
b ALERT c For initiation of therapy, No dose adjustment.
must have WBC equal to or greater than
3,500 cells/mm3 and ANC equal to or SIDE EFFECTS
greater than 1,500 cells/mm3. 1,000 cells/ Frequent (39%–14%): Drowsiness, sali-
mm3 or greater in pts with documented vation, tachycardia, dizziness, constipa-
benign ethnic neutropenia (BEN). tion. Occasional (9%–4%): Hypotension,
Canadian trade name Non-Crushable Drug High Alert drug
268 cobimetinib
headache, tremor, syncope, diaphoresis,
dry mouth, nausea, visual disturbances, cobimetinib
nightmares, restlessness, akinesia, agita-
C tion, hypertension, abdominal discomfort, koe-bi-me-ti-nib
heartburn, weight gain. Rare: Rigidity, con- (Cotellic)
fusion, fatigue, insomnia, diarrhea, rash. Do not confuse cobimetinib
with cabozantinib, imatinib, or
ADVERSE EFFECTS/TOXIC trametinib.
REACTIONS
uCLASSIFICATION
Seizures occur occasionally (3% of pts).
Overdose produces CNS depression PHARMACOTHERAPEUTIC: MEK in-
(sedation, delirium, coma), respira- hibitor. CLINICAL: Antineoplastic.
tory depression, hypersalivation. Blood
dyscrasias, particularly agranulocytosis,
USES
mild leukopenia, may occur.
Treatment of pts with unresectable or
NURSING CONSIDERATIONS metastatic melanoma with a BRAF V600E
or V600K mutation, in combination with
BASELINE ASSESSMENT vemurafenib.
Obtain baseline weight, glucose, Hgb
A1c, WBC, absolute neutrophil count PRECAUTIONS
(ANC) before initiating treatment. Assess Contraindications: Hypersensitivity to
behavior, appearance, emotional status, cobimetinib. Cautions: Baseline ane-
response to environment, speech pattern, mia, lymphopenia, thrombocytopenia;
thought content. cardiomyopathy, hepatic/renal impair-
INTERVENTION/EVALUATION
ment, HF, hypertension, ocular disor-
ders; pts at risk for bleeding (history
Monitor B/P for hypertension/hypo- of gastrointestinal, genitourinary, in-
tension. Assess pulse for tachycardia tracranial, reproductive system bleed-
(common side effect). Monitor CBC for ing), electrolyte imbalance. Not rec-
blood dyscrasias. Monitor ANC, WBC ommended in pts taking moderate or
count every wk for first 6 mos, then strong CYP3A inhibitors.
biweekly for 6 mos. If CBC and ANC
are normal after 12 mos, then monthly ACTION
monitoring of CBC and ANC is recom- Potent and selective inhibitor of mitogen-
mended. Supervise suicidal-risk pt activated extracellular kinase (MEK)
closely during early therapy (as depres- pathway. Reversibly inhibits MEK1 and
sion lessens, energy level improves, MEK2, which are upstream regulators
increasing suicide potential). Assess of the ERK pathway. The ERK pathway
for therapeutic response (interest in promotes cellular proliferation. MEK1
surroundings, improvement in self- and MEK2 are part of the BRAF path-
care, increased ability to concentrate, way. Therapeutic Effect: Increases
relaxed facial expression). apoptosis and reduces tumor growth.
PATIENT/FAMILY TEACHING
PHARMACOKINETICS
• Do not abruptly discontinue long-term
drug therapy. • Avoid tasks that require Widely distributed. Metabolized in
alertness, motor skills until response to liver. Protein binding: 95%. Peak
drug is established. • Drowsiness gen- plasma concentration: 2.4 hrs. Steady
erally subsides during continued ther- state reached in 9 days. Eliminated
apy. • Avoid alcohol, caffeine. • Re- in feces (76%), urine (18%). Half-
port fever, sore throat, flu-like symptoms. life: 44 hrs.

underlined – top prescribed drug


cobimetinib 269

LIFESPAN CONSIDERATIONS Concomitant Use of CYP3A Inhibitors


Reduce dose to 20 mg once daily if short-
Pregnancy/Lactation: Avoid preg-
term (14 days or less) use of moderate
nancy; may cause fetal harm/malforma-
tions. Female pts of reproductive poten-
CYP3A inhibitors is unavoidable. May C
resume 60-mg once-daily dose once the
tial should use effective contraception
short-term CYP3A inhibitor is discontin-
during treatment and up to 2 wks after
ued. Use an alternative strong or moder-
discontinuation. Unknown if distributed
ate CYP3A inhibitor in pts already taking
in breast milk. Breastfeeding not recom-
reduced dose of 20 mg or 40 mg daily.
mended. May reduce fertility in females
and males. Children/Elderly: Safety Dose Modification
and efficacy not established. Based on Common Terminology Criteria for
Adverse Events (CTCAE) grading 1–4. See
INTERACTIONS prescribing information for vemurafenib
DRUG: Strong CYP3A inhibitors for recommended dose modification.
(e.g., clarithromycin, ketoconazole,
ritonavir), moderate CYP3A inhibi- Dose Reduction Schedule
tors (e.g., atazanavir, ciprofloxa- First dose reduction: 40 mg once
cin) may increase concentration/effect. daily. Second dose reduction: 20 mg
Strong CYP3A inducers (e.g., car- once daily. Permanently discontinue if
BAMazepine, rifampicin), moder- unable to tolerate 20 mg once daily.
ate CYP3A inducers (e.g., bosentan,
nafcillin) may decrease concentration/ Cardiomyopathy
effect. HERBAL: St. John’s wort may de- Asymptomatic decrease in left
crease concentration/effect. FOOD: None ventricular ejection fraction (LVEF)
known. LAB VALUES: Many increase greater than 10% from baseline and
serum alkaline phosphatase, ALT, AST, less than institutional lower limit of
creatine phosphokinase, creatinine, GGT. normal (LLN): Withhold treatment for
May decrease Hct, Hgb, lymphocytes, 2 wks, then reassess LVEF. Resume at next
platelets, RBCs; serum albumin, calcium, lower dose level if LVEF is at or above LLN
sodium. May increase or decrease serum and the decrease from baseline is 10%
potassium. or less. Permanently discontinue if LVEF
is less than LLN or the decrease from
AVAILABILITY (Rx) baseline LVEF is more than 10%. Symp-
Tablets: 20 mg. tomatic decrease of LVEF from base-
line: Withhold treatment for up to 4 wks,
ADMINISTRATION/HANDLING then reassess LVEF. Resume at next lower
PO dose level if symptoms resolve, LVEF is at
• Give without regard to food. • If or above LLN, and the decrease from base-
dose is missed or vomiting occurs during line LVEF is 10% or less. Permanently dis-
administration, give next dose at regu- continue if symptoms persist, LVEF is less
larly scheduled time. than LLN, or the decrease from baseline
LVEF is more than 10%.
INDICATIONS/ROUTES/DOSAGE
Dermatologic Reactions
Metastatic Melanoma
Grade 2 (intolerable); Grade 3 or
PO: ADULTS, ELDERLY: 60 mg (three 20-
4: Withhold or reduce dose.
mg tablets) once daily for first 21 days of
28-day cycle (in combination with vemu- Hepatotoxicity or Hepatic Laboratory
rafenib). Continue until disease progres- Abnormalities
sion or unacceptable toxicity. First occurrence, Grade 4: Withhold
treatment for up to 4 wks. If improved

Canadian trade name Non-Crushable Drug High Alert drug


270 cobimetinib
to Grade 0 or 1, resume at next lower Renal Impairment
dose level. If not improved to Grade 0 or Mild to moderate impairment: No
1 within 4 wks, permanently discontinue. dose adjustment. Severe impair-
C Recurrent Grade 4: Permanently dis- ment: Not specified; use caution.
continue.
Hepatic Impairment
Hemorrhage Mild impairment: No dose adjust-
Grade 3: Withhold treatment for up to ment. Moderate to severe impair-
4 wks. If not improved to Grade 0 or 1, ment: Not specified; use caution.
resume at next lower dose level. If not
improved within 4 wks, permanently SIDE EFFECTS
discontinue. Grade 4: Permanently dis- Frequent (60%–24%): Diarrhea, photosensi-
continue. tivity, sunburn, solar dermatitis, nausea, py-
rexia, vomiting. Occasional (16%–10%): Ac-
New Primary Malignancies neiform dermatitis, stomatitis, aphthous
(Cutaneous or Noncutaneous) stomatitis, mouth ulceration, mucosal in-
No dose adjustment. flammation, alopecia, hypertension, vision
impairment, blurred vision, reduced visual
Nonspecific Adverse Effects acuity, hyperkeratosis, erythema, chills.
Any intolerable Grade 2; any Grade
3: Withhold for up to 4 wks. If improved ADVERSE EFFECTS/TOXIC
to Grade 0 or 1, resume at next lower dose REACTIONS
level. If not improved within 4 wks, perma- Anemia, lymphopenia, thrombocytopenia
nently discontinue. First occurrence of is an expected response to therapy. New
any Grade 4: Permanently discontinue. primary malignancies, including squamous
Ocular Toxicities
cell carcinoma, keratoacanthoma, second-
Serious retinopathy: Withhold treat- ary-primary melanomas, were reported.
ment for up to 4 wks. If signs and symp- Serious, sometimes fatal hemorrhagic
toms improve, resume at next lower dose events, including GI bleeding (4% of pts),
level. If not improved or symptoms recur intracranial bleeding (1% of pts), hematu-
at the lower dose within 4 wks, perma- ria (2% of pts), reproductive system hem-
nently discontinue. Retinal vein occlu- orrhage (2% of pts), have occurred. Other
sion: Permanently discontinue.
hemorrhagic events may include cerebral/
conjunctival/intracranial/gingival/hemor-
Photosensitivity rhoidal/ovarian/pulmonary/rectal/uterine/
Grade 2 (intolerable); Grade 3 or vaginal bleeding; ecchymosis, epistaxis.
4: Withhold treatment for up to 4 wks. If Grade 3 or 4 cardiomyopathy reported in
improved to Grade 0 or 1, resume at next 26% of pts. Grade 3 or 4 skin reactions
lower dose level. If not improved within 4 including severe rash occurred in 16% of
wks, permanently discontinue. pts. Ocular toxicities, including retinopa-
thy, chorioretinopathy, retinal detachment,
Rhabdomyolysis, CPK Level Elevations reported in 26% of pts. Grade 3 or 4 CPK
Grade 4 CPK elevation or any CPK level elevations occurred in 14% of pts and
elevation with myalgia: Withhold may lead to rhabdomyolysis. Hepatotoxicity
treatment for up to 4 wks. If improved to reported in 7%–11% of pts. Severe photo-
Grade 3 or lower, resume at next lower sensitivity reported in 47% of pts.
dose level. If not improved within 4 wks,
permanently discontinue. NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Severe Hypersensitivity Reaction
Permanently discontinue. Confirm presence of BRAF V600E or
V600K mutation in tumor specimen prior
underlined – top prescribed drug
colchicine 271
to initiation. Obtain baseline CBC, BMP, flank pain, dark-colored urine, decreased
LFT, CPK; serum albumin, magnesium, urinary output; strokelike symptoms; new
phosphate, ionized calcium; urine preg- skin moles or lesions, rash; eye pain, vi-
nancy; vital signs. Obtain ophthalmologic sion changes; heart problems such as C
exam with visual acuity; ECG, echocar- shortness of breath, dizziness, fainting,
diogram for LVEF. Assess skin for moles, palpitations. • Report any newly pre-
lesions, papillomas. Verify use of effective scribed medications. • Avoid sunlight,
contraception in female pts of reproduc- tanning beds. Wear protective clothing,
tive potential. Receive full medication his- high-SPF sunscreen, and lip balm when
tory, including herbal products. Question outdoors. • Treatment may cause fetal
history as listed in Precautions. Assess harm. Women of childbearing potential
hydration status. should use effective contraception during
treatment and up to 2 wks after last dose.
INTERVENTION/EVALUATION
Immediately report suspected pregnancy.
Monitor CBC, BMP, LFT, CPK; serum al- Do not breastfeed. Treatment may reduce
bumin, magnesium, phosphate, ionized fertility.
calcium; vital signs. Assess skin for new
lesions, dermal toxicities at least q2mos
during treatment and for least 6 mos af-
ter discontinuation. Assess LVEF by echo- colchicine
cardiogram 1 mo after initiation, then
q3mos thereafter until discontinuation. kol-chi-seen
If treatment interrupted due to change in (Colcrys, Mitigare)
LVEF, monitor LVEF at 2 wks, 4 wks, 10 Do not confuse colchicine with
wks, and 16 wks, and then as indicated. Cortrosyn.
Conduct ophthalmologic examinations
regularly, esp. with any new or worsen- uCLASSIFICATION
ing visual disturbances. Assess for eye PHARMACOTHERAPEUTIC: Alkaloid.
pain, visual changes. Immediately report CLINICAL: Antigout.
GI bleeding, hematuria, unusual repro-
ductive system hemorrhage; symptoms
of intracranial bleeding (aphasia, blind- USES
ness, confusion, facial droop, hemiple- Prevention, treatment of acute gouty ar-
gia, seizures). Monitor for hepatotoxic- thritis. Used to reduce frequency of re-
ity; monitor for signs of rhabdomyolysis, currence of familial Mediterranean fever
such as dark-colored urine, flank pain, (FMF) in adults and children 4 yrs and
decreased urine output, muscle aches. older. OFF-LABEL: Treatment of biliary
Due to high risk of diarrhea, strictly cirrhosis, recurrent pericarditis.
monitor I&O.
PRECAUTIONS
PATIENT/FAMILY TEACHING
Contraindications: Hypersensitivity to
• Blood levels monitoring, cardiac func- colchicine. Concomitant use of a P-glyco-
tion tests, eye exams, skin exams will be protein (e.g., cycloSPORINE) or strong
conducted frequently. • Treatment may CYP3A4 inhibitor (e.g., clarithromycin)
lead to severe anemia, HF, kidney failure, in presence of renal or hepatic impair-
new cancers, severe light sensitivity, liver ment. Mitigare: Pts with both renal/
dysfunction, skin toxicities (such as se- hepatic impairment. Cautions: Hepatic
vere rash, peeling), vision changes. • impairment, elderly, debilitated pts, renal
Report bloody stools, bloody urine, un- impairment. Concomitant use of cyclo-
usual reproductive system bleeding, nose- SPORINE, diltiaZEM, verapamil, fibrates,
bleeds, coughing up blood; abdominal or statins may increase risk of myopathy.

Canadian trade name Non-Crushable Drug High Alert drug


272 colchicine

ACTION ADMINISTRATION/HANDLING
Disrupts cytoskeletal functions by pre- PO
venting activation, degranulation, and • Give without regard to food. • For FMF,
C migration of neutrophils associated with give in 1 or 2 divided doses. • Give with
gout symptoms. In FMF, may interfere adequate water and maintain fluid intake.
with intracellular assembly of inflamma-
some complex present in neutrophils and INDICATIONS/ROUTES/DOSAGE
monocytes. Therapeutic Effect: Re- Acute Gouty Arthritis (Colcrys)
duces inflammatory process. PO: ADULTS, ELDERLY: Initially, 1.2 mg
at first sign of gout flare, then 0.6 mg
PHARMACOKINETICS 1 hr later. Maximum: 1.8 mg within
Rapidly absorbed from GI tract. Oral bio- 1 hr. Coadministration with strong
availability: 45%. Highest concentration CYP3A4 inhibitors: Initially, 0.6 mg,
is in liver, spleen, kidney. Protein bind- then 0.3 mg dose 1 hr later. Do not re-
ing: 30%–50%. Re-enters intestinal tract peat for at least 3 days. Coadministra-
by biliary secretion and is reabsorbed tion with moderate CYP3A4 inhibi-
from intestines. Partially metabolized in tors: 1.2 mg once. Do not repeat for
liver via CYP3A4. Eliminated primarily in at least 3 days. Coadministration with
feces. Half-life: 27–31 hrs. P-glycoprotein inhibitors: 0.6 mg
once. Do not repeat for at least 3 days.
LIFESPAN CONSIDERATIONS
Gout Prophylaxis (Colcrys, Mitigare)
Pregnancy/Lactation: Drug crosses
placenta and is distributed in breast milk. Note: Duration of prophylaxis is 6 mos
Children: Safety and efficacy not estab-
or 3 mos (pts without tophi) to 6 mos
lished. Elderly: May be more suscep- (pts with 1 or more tophi)
PO: ADULTS, ELDERLY: 0.6 mg 1–2 times/
tible to cumulative toxicity. Age-related
renal impairment may increase risk of day. Maximum: 1.2 mg/day. Coadmin-
myopathy. istration with strong CYP3A4 inhibi-
tors: If dose is 0.6 mg 2 times/day, adjust
INTERACTIONS dose to 0.3 mg once daily; if dose is 0.6
mg once daily, adjust dose to 0.3 mg ev-
DRUG: CYP3A4 inhibitors (e.g., clar- ery other day. Coadministration with
ithromycin, dilTIAZem, ketocon- moderate CYP3A4 inhibitors: If dose
azole, ritonavir), P-glycoprotein/ is 0.6 mg 2 times/day, adjust dose to 0.3
ABCB1 inhibitors (e.g. amioda- mg twice daily or 0.6 mg once daily; if dose
rone) may increase concentration/ef- is 0.6 mg once daily, adjust dose to 0.3
fect. May increase concentration/effect; mg once daily. Coadministration with
risk of adverse effects (myopathy) of P-glycoprotein inhibitors: If dose is
HMG-CoA inhibitors (statins) (e.g., 0.6 mg 2 times/day, adjust dose to 0.3 mg
atorvastatin). HERBAL: None signifi- once daily; if dose is 0.6 mg once daily, ad-
cant. FOOD: Grapefruit products may just dose to 0.3 mg every other day.
increase concentration/toxicity. LAB VAL-
UES: May increase serum alkaline phos- FMF (Colcrys)
phatase, AST. May decrease platelet count. PO: ADULTS, ELDERLY, CHILDREN OLDER
THAN 12 YRS: 1.2–2.4 mg/day in 1–2 di-
AVAILABILITY (Rx) vided doses. Titrate dose in 0.3-mg incre-
Tablets: (Colcrys): 0.6 mg. Capsule: ments. Coadministration with strong
(Mitigare): 0.6 mg. CYP3A4 inhibitors: Maximum: 0.6
mg once daily (or 0.3 mg twice daily).
Coadministration with moderate
CYP3A4 inhibitors: 1.2 mg/day (0.6

underlined – top prescribed drug


conjugated ­estrogens 273
mg twice daily). Coadministration with abdominal pain, fever, chills, erythema,
P-glycoprotein inhibitors: 0.6 mg swollen skin lesions.
once daily (or 0.3 mg twice daily). CHIL-
INTERVENTION/EVALUATION C
DREN 6–12 YRS: 0.9–1.8 mg/day in 1–2
divided doses. CHILDREN 4–5 YRS: 0.3–1.8 Discontinue medication immediately if GI
mg/day in 1–2 divided doses. Note: In- symptoms occur. Encourage high fluid
crease or decrease dose by 0.3 mg/day, intake (3,000 mL/day). Monitor I&O
not to exceed maximum dose. (output should be at least 2,000 mL/day),
CBC, hepatic/renal function tests. Monitor
Pericarditis serum uric acid. Assess for therapeutic
PO: ADULTS, ELDERLY: 0.6 mg 2 times/ response: relief of pain, stiffness, swelling;
day. increased joint mobility; reduced joint ten-
derness; improved grip strength.
Dosage in Renal Impairment
Creatinine Clearance Dosage PATIENT/FAMILY TEACHING
Less than 30 mL/min • Drink 8–10 (8-oz) glasses of fluid
FMF 0.3 mg initially daily while taking medication. • Report
Gout prophylaxis 0.3 mg/day skin rash, sore throat, fever, unusual
Gout flare No reduction bruising/bleeding, weakness, fatigue,
HD numbness. • Stop medication as soon
FMF 0.3 mg as single as gout pain is relieved or at first sign of
dose
Gout prophylaxis 0.3 mg 2–4
nausea, vomiting, diarrhea. • Avoid
times/wk grapefruit products.

Dosage in Hepatic Impairment


Use caution. conjugated
SIDE EFFECTS ­estrogens
Frequent: Nausea, vomiting, abdomi-
nal discomfort. Occasional: Anorexia. kon-joo-gate-ed ess-troe-jenz
Rare: Hypersensitivity reaction, includ- (Premarin)
ing angioedema. j BLACK BOX ALERT jRisk of
dementia may be increased in post-
ADVERSE EFFECTS/TOXIC menopausal women. Do not use to
prevent cardiovascular disease.
REACTIONS May increase risk of endometrial
Bone marrow depression (aplastic ane- carcinoma or invasive breast can-
mia, agranulocytosis, thrombocytopenia) cer in postmenopausal women.
may occur with long-term therapy. Over- Do not confuse Premarin with
dose initially causes burning feeling in Primaxin, Provera, or Remeron.
skin/throat; severe diarrhea, abdominal
pain. Second stage manifests as fever, FIXED-COMBINATION(S)
seizures, delirium, renal impairment Duavee: conjugated estrogen/baze-
(hematuria, oliguria). Third stage causes doxifene (estrogen agonist/antago-
hair loss, leukocytosis, stomatitis. nist): 0.45 mg/20 mg.

NURSING CONSIDERATIONS uCLASSIFICATION


PHARMACOTHERAPEUTIC: Estro-
BASELINE ASSESSMENT
gen. CLINICAL: Hormone.
Obtain baseline laboratory studies. Gout:
Assess involved joints for pain, mobility,
edema. Mediterranean fever: Assess

Canadian trade name Non-Crushable Drug High Alert drug


274 conjugated ­estrogens

USES LIFESPAN CONSIDERATIONS


Management of moderate to severe vaso- Pregnancy/Lactation: Distributed
motor symptoms associated with meno- in breast milk. May cause fetal harm.
C pause. Treatment of hypoestrogenism due Breastfeeding not recommended. Chil-
to hypogonadism, castration, or primary dren: Safety and efficacy not established.
ovarian failure. Prevention of osteoporo- Elderly: No age-related precautions noted.
sis in postmenopausal women. Palliative
­treatment of inoperable, progressive can- INTERACTIONS
cer of the prostate and breast in men, and DRUG: May decrease therapeutic ef-
of the breast in postmenopausal women. fect of anticoagulants (e.g., war-
Abnormal uterine bleeding (injection farin), anastrozole, exemestane.
only). Treatment of moderate to severe HERBAL: Herbals with estrogenic
vulvar and vaginal atrophy due to meno- properties (e.g., fennel, red clover,
pause. OFF-LABEL: Prevention of estrogen ginseng) may increase adverse effects.
deficiency–induced premenopausal osteo- FOOD: Grapefruit products may in-
porosis. Cream: Prevention of nosebleeds. crease concentration/toxicity. LAB VAL-
UES: May increase serum glucose, HDL,
PRECAUTIONS calcium, triglycerides. May decrease se-
Contraindications: Hypersensitivity to es- rum cholesterol, LDH. May affect serum
trogens. Breast cancer (except in pts being metapyrone testing, thyroid function tests.
treated for metastatic disease), hepatic dis-
ease, history of or current thrombophlebi- AVAILABILITY (Rx)
tis, undiagnosed abnormal vaginal bleeding, Cream, Vaginal: (Premarin): 0.625 mg/g.
pregnancy, DVT or PE (current or history Injection, Powder for Reconstitution: 25
of), angioedema or anaphylactic reaction mg. Tablets: 0.3 mg, 0.45 mg, 0.625 mg,
to estrogens, estrogen-dependent tumors. 0.9 mg, 1.25 mg.
Known protein C, protein S, antithrombin
deficiency or other thrombophilic disor- ADMINISTRATION/HANDLING
der. Cautions: Asthma, epilepsy, migraine IV
headaches, diabetes, cardiac/renal dysfunc-
tion, history of severe hypocalcemia, lupus Reconstitution • Reconstitute with
erythematosus, porphyria, endometriosis, Sterile Water for Injection. • Slowly
gallbladder disease, familial defects of lipo- add diluent, shaking gently. • Avoid vig-
protein metabolism. Hypoparathyroidism, orous shaking.
history of cholestatic jaundice. Rate of administration • Give slowly
to prevent flushing reaction.
ACTION Storage • Refrigerate vials for IV
Responsible for development and mainte- use. • Use immediately following re-
nance of female reproductive system and constitution.
secondary sexual characteristics; modu-
lates release of gonadotropin-releasing PO
hormone, reduces follicle-stimulating hor- • Administer at same time each day. • Give
mone (FSH), luteinizing hormone (LH). with milk, food if nausea occurs.
Therapeutic Effect: Reduces elevated
levels of gonadotropins, LH, and FSH. IV INCOMPATIBILITIES
No information available on Y-site admin-
PHARMACOKINETICS istration.
Well absorbed from GI tract. Widely dis-
tributed. Protein binding: 50%–80%. INDICATIONS/ROUTES/DOSAGE
Metabolized in liver. Primarily excreted in Note: Cyclic administration is either 3
urine. Half-life (total estrone): 27 hrs. wks on, 1 wk off or 25 days on, 5 days off.
underlined – top prescribed drug
conjugated ­estrogens 275
Vasomotor Symptoms Associated with SIDE EFFECTS
Menopause
Frequent: Vaginal bleeding (spotting,
PO: ADULTS, ELDERLY: 0.3 mg/day cycli-
breakthrough bleeding), breast pain/ten-
cally or daily. derness, gynecomastia. Occasional: Head- C
Vulvar and Vaginal Atrophy ache, hypertension, intolerance to contact
PO: ADULTS, ELDERLY: 0.3 mg/day cycli- lenses. High doses: Anorexia, nausea.
cally or daily. Rare: Loss of scalp hair, depression.
Intravaginal: ADULTS, ELDERLY: 0.5–2 ADVERSE EFFECTS/TOXIC
g/day cyclically. REACTIONS
Hypoestrogenism due to Hypogonadism Prolonged administration may increase
PO: ADULTS: 0.3–0.625 mg/day given cy- risk of breast, cervical, endometrial,
clically. Dose may be titrated in 6- to 12- hepatic, vaginal carcinoma; cerebrovas-
mo intervals. Progestin treatment should cular disease, coronary heart disease,
be added to maintain bone mineral den- gallbladder disease, hypercalcemia.
sity once skeletal maturity is achieved.
NURSING CONSIDERATIONS
Hypoestrogenism due to Castration,
BASELINE ASSESSMENT
Primary Ovarian Failure
PO: ADULTS: Initially, 1.25 mg/day cycli- Question for hypersensitivity to estrogen,
cally. Adjust dosage, upward or down- hepatic impairment, thromboembolic
ward, according to severity of symptoms disorders associated with pregnancy, es-
and pt response. For maintenance, adjust trogen therapy. Assess frequency/severity
dosage to lowest level that will provide ef- of vasomotor symptoms. Review results
fective control. of baseline mammogram in pts with
breast cancer.
Postmenopausal Osteoporosis Prevention
INTERVENTION/EVALUATION
PO: ADULTS, ELDERLY: 0.3 daily or cycli-
cally. Assess B/P periodically. Assess for edema;
weigh daily. Monitor for loss of vision,
Breast Cancer (Metastatic) diplopia, migraine, thromboembolic dis-
PO: ADULTS, ELDERLY: 10 mg 3 times/day order, sudden onset of proptosis.
for at least 3 mos. PATIENT/FAMILY TEACHING
Prostate Cancer (Advanced) • Avoid smoking due to increased risk
PO: ADULTS, ELDERLY: 1.25–2.5 mg 3 of heart attack, blood clots. • Avoid
times/day. grapefruit products. • Diet, exercise
important part of therapy when used to
Abnormal Uterine Bleeding retard osteoporosis. • Promptly report
IV, IM: ADULTS: 25 mg; may repeat signs/symptoms of thromboembolic,
once in 6–12 hrs. thrombotic disorders: sudden severe
headache, shortness of breath, vision/
Dyspareunia speech disturbance, weakness/numbness
Intravaginal: ADULTS, ELDERLY: 0.5 g of an extremity, loss of coordination; pain
cyclically (21 days on, 7 days off) or 0.5 in chest, groin, leg. • Report abnormal
g twice weekly. vaginal bleeding, depression. • Teach
female pts to perform breast self-
Dosage in Renal Impairment
exam. • Report weight gain of more
No dose adjustment.
than 5 lbs a wk. • Stop taking medica-
Dosage in Hepatic Impairment tion, contact physician if pregnancy is
Contraindicated. suspected.

Canadian trade name Non-Crushable Drug High Alert drug


276 copanlisib
of contraception (failure rate less than 1%
copanlisib per yr) during treatment and for at least 1
mo after discontinuation. Unknown if dis-
C koe-pan-lis-ib tributed in breast milk. Breastfeeding not
(Aliqopa) recommended during treatment and for
Do not confuse copanlisib with at least 1 mo after discontinuation. May
cabozantinib, cobimetinib, impair fertility in females and males of
duvelisib or idelalisib. reproductive potential. Males: Must use
condoms during treatment and up to 1 mo
uCLASSIFICATION
after treatment, despite prior history of va-
PHARMACOTHERAPEUTIC: Phos- sectomy. Children: Safety and efficacy not
phatidylinositol 3-kinase inhibitor. established. Elderly: No age-related pre-
CLINICAL: Antineoplastic. cautions noted.
INTERACTIONS
USES
DRUG: Strong CYP3A4 inhibitors
Treatment of adults with relapsed follicu- (e.g., clarithromycin, ketoconazole,
lar lymphoma who have received at least ritonavir) may increase concentration/
two prior systemic therapies. effect. Strong CYP3A4 inducers (e.g.,
rifAMPin, phenytoin, carBAMaze-
PRECAUTIONS
pine) may decrease concentration/effect.
Contraindications: Hypersensitivity to May decrease effect of BCG (intravesi-
copanlisib. Cautions: Baseline anemia, cal). May enhance adverse/toxic effects
leukopenia, lymphopenia, neutropenia, of natalizumab, pimecrolimus, tacro-
thrombocytopenia; active infection, con- limus, vaccines (live). HERBAL: Echi-
ditions predisposing to infection (e.g., nacea, St. John’s wort may decrease
diabetes, renal failure, immunocompro- concentration/effect. FOOD: Grapefruit
mised pts, open wounds); history of dia- products may increase concentration/
betes, hypertension, pulmonary disease. effect. LAB VALUES: May increase serum
Concomitant use of moderate CYP3A glucose, lipase, triglycerides, uric acid.
inhibitors. May decrease Hgb, lymphocytes, neutro-
phils, platelets, WBC; serum phosphate.
ACTION
Inhibits phosphatidylinositol-3-kinase AVAILABILITY (Rx)
(PI3K) expressed on malignant B-cells. Injection, Lyophilized Solid for Reconstitu-
Inhibits signaling pathway of B-cell tion: 60 mg.
receptors, lymphoma cells lines, and
CXCR12-mediated chemotaxis of malig- ADMINISTRATION/HANDLING
nant B-cells. Therapeutic Effect: In-
IV
hibits tumor cell growth and metastasis.
Induces cellular death by apoptosis. Reconstitution • Reconstitute lyophi-
lized solid using 4.4 mL of 0.9% NaCl for
PHARMACOKINETICS a vial concentration of 15 mg/
Widely distributed. Metabolized in liver. mL. • Gently shake vial for 30
Protein binding: 84%. Excreted in feces secs. • Allow vial to settle for 1 min
(64%), urine (22%). Half-life: 39 hrs. (allowing bubbles to rise to sur-
face). • If any contents are not com-
LIFESPAN CONSIDERATIONS pletely dissolved, repeat gentle shaking
Pregnancy/Lactation: Avoid pregnancy; and settling process. • Visually inspect
may cause fetal harm. Females of repro- for particulate matter or discoloration.
ductive potential must use reliable form Solution should appear colorless to

underlined – top prescribed drug


copanlisib 277
slightly yellow in color. Do not use if so- occurrences: Withhold treatmentuntil
lution is cloudy, discolored, or visible fasting glucose is 160 mg/mL or less, or
particles are observed. • For 60 mg until random/nonfasting glucose is 200
dose, withdraw 4 mL of solution from mg/mL or less. Then, reduce dose to 30 C
vial. For 45 mg dose, withdraw 3 mL of mg dose. If hyperglycemia persists at 30
solution from vial. For 30 mg dose, with- mg dose, permanently discontinue.
draw 2 mL of solution from vial. • Di-
lute solution in 100 mL of 0.9% Hypertension
NaCl. • Mix by gentle inversion. B/P 150/90 mmHg or greater (pre-
Rate of administration • Infuse over dose): Withhold treatment until two con-
60 mins. secutive B/P measurements (at least 15
Storage • Refrigerate unused vi- min apart) are less than 150/90 mmHg.
als. • May refrigerate reconstituted vial Non–life-threatening B/P 150/90
or diluted solution for up to 24 hrs. • If mmHg or greater (post-dose): Con-
refrigerated, allow diluted solution to tinue at same dose if antihypertensive
warm to room temperature before infu- therapy is not indicated. If antihyper-
sion. • Avoid direct sunlight. tensive therapy is indicated, consider
dose reduction from 60 mg to 45 mg,
IV COMPATIBILITIES/ or from 45 mg to 30 mg. If B/P remains
INCOMPATIBILITIES 150/90 mmHg or higher at 30 mg dose
Reconstitute and dilute using only 0.9% despite antihypertensive therapy, perma-
NaCl. Do not infuse with other medications. nently discontinue. Life-threatening
B/P 150/90 mmHg or greater (post-
INDICATIONS/ROUTES/DOSAGE dose): Permanently discontinue.
Follicular Lymphoma Infection
IV: ADULTS, ELDERLY: 60 mg on days 1, 8, Grade 3 or higher infection: With-
and 15 of a 28-day cycle on an intermit- hold treatment until resolved. Sus-
tent schedule (3 wks on, 1 wk off). Con- pected Pneumocystis jiroveci
tinue until disease progression or unac- pneumonia (PJP) infection of any
ceptable toxicity. grade: Withhold treatment. If PJP in-
Dose Modification fection is confirmed, treat infection until
Based on Common Terminology Criteria resolved. Then, resume treatment at same
for Adverse Events (CTCAE). dose with concomitant PJP preventative
therapy.
Hyperglycemia
Neutropenia
Fasting serum blood glucose level
Absolute neutrophil count (ANC)
equal to 160 mg/mL or greater (pre-
less than 500 cells/mm3: Withhold
dose): Withhold treatment until fasting
serum glucose is 160 mg/mL or less. treatment until ANC is 500 cells/mm3 or
Random/nonfasting blood glucose
greater, then resume at same dose. Re-
currence of ANC 500 cells/mm3 or
level equal to 200 mg/mL or greater:
less: Reduce dose to 45 mg.
Withhold treatment until random/non-
fasting glucose is 200 mg/mL or less. Noninfectious Pneumonitis
Serum blood glucose level equal to Grade 2 noninfectious pneumonitis
500 mg/mL or greater (pre-dose or (NIP): Withhold treatment and treat NIP.
post-dose): First occurrence: With- Once recovered to Grade 1 or 0, reduce
hold treatment until fasting glucose is 160 dose at 45 mg dose. If Grade 2 NIP re-
mg/mL or less, or until random/nonfast- curs, permanently discontinue. Grade 3
ing glucose is 200 mg/mL or less. Then, or higher noninfectious pneumoni-
reduce dose to 45 mg dose. Sub­sequent tis (NIP): Permanently discontinue.

Canadian trade name Non-Crushable Drug High Alert drug


278 copanlisib
Severe Cutaneous Reactions aspergillosis, lung infection reported in
Grade 3 severe cutaneous reac- 21% of pts. Pneumocystis jiroveci pneu-
tions: Withhold treatment until re- monia reported in less than 1% of pts.
C solved, then reduce dose from 60 mg to Hyperglycemia reported 54% of pts. Blood
45 mg, or from 45 mg to 30 mg. Life- glucose levels usually peaked 5–8 hrs af-
threatening severe cutaneous reac- ter infusion. CTCAE Grade 3 hypertension
tions: Permanently discontinue. occurred in 26% of pts. Noninfectious
pneumonitis occurred in 5% of pts. Severe
Thrombocytopenia
cutaneous reactions reported in 3% of pts.
Platelet count less than 25,000
cells/mm3: Withhold treatment until NURSING CONSIDERATIONS
platelet count is 75,000 cells/mm3 or
greater. If recovery occurs within 21 BASELINE ASSESSMENT
days, reduce dose from 60 mg to 45 Obtain ANC, CBC, vital signs. Screen for
mg, or from 45 mg to 30 mg. If recovery active infection. Obtain pregnancy test in
does not occur within 21 days, perma- females of reproductive potential. Ques-
nently discontinue. tion current breastfeeding status. Confirm
Other Toxicities
compliance of effective contraception.
Any other Grade 3 toxicities: With- Question history of diabetes, hyperten-
hold treatment until resolved, then re- sion, pulmonary disease. Pts with history
duce dose from 60 mg to 45 mg, or from of diabetes, hypertension should have
45 mg to 30 mg. adequate control prior to initiation. Re-
ceive full medication history and screen
Concomitant Use of Strong CYP3A for interactions. Offer emotional support.
Inhibitors
If strong CYP3A inhibitor cannot be dis- INTERVENTION/EVALUATION
continued, reduce dose to 45 mg. Monitor ANC, CBC, platelet count periodi-
cally. Monitor blood glucose level prior
Dosage in Renal Impairment to each treatment; B/P before and after
Mild to moderate impairment: No each treatment. Be alert for infections,
dose adjustment. Severe impair- esp. lower respiratory tract infection such
ment: Not specified; use caution. as pneumocystis jiroveci pneumonia,
Dosage in Hepatic Impairment
bacterial/fungal/pneumococcal/viral
Mild impairment: No dose adjust-
pneumonia (cough, dyspnea, hypoxia,
ment. Moderate to severe impair- pleuritic chest pain). Consider ABG, ra-
ment: Not specified; use caution.
diologic test if lung infection or pneumo-
nitis suspected. If treatment-related toxic-
SIDE EFFECTS ities occur, consider referral to specialist.
Frequent (36%): Fatigue, asthenia, di-
Assess skin for cutaneous reactions.
arrhea. Occasional (15%–7%): Rash, PATIENT/FAMILY TEACHING
stomatitis, oropharyngeal erosion, oral • Treatment may depress your immune
pain, vomiting, mucosal inflammation, system and reduce your ability to fight
paresthesia, dysesthesia. infection. Report symptoms of infection
ADVERSE EFFECTS/TOXIC such as body aches, chills, cough, fa-
REACTIONS tigue, fever. Avoid those with active infec-
tion. • Report symptoms of high blood
Anemia, leukopenia, lymphopenia, neu- sugar levels (confusion, excessive thirst/
tropenia, thrombocytopenia is expected hunger, headache, frequent urination);
response to therapy. Serious infections high blood pressure (dizziness, head-
including bacterial/fungal/pneumococ- ache, fainting); inflammation of the lung
cal/viral pneumonia, bronchopulmonary
underlined – top prescribed drug
crizotinib 279
(excessive cough, difficulty breathing); tais (RON). ALK gene abnormalities due
toxic skin reactions (itching, peeling, to mutation may result in expression of
rash, redness, swelling). • Females and oncogenic fusion proteins. Therapeutic
males of reproductive potential must use Effect: Inhibits tumor cell proliferation C
reliable contraception during treatment of cells expressing genetic alteration.
and for at least 1 mo after last dose.
Treatment may cause fetal harm. • Do PHARMACOKINETICS
not breastfeed during treatment and for Well absorbed after PO administration.
at least 1 mo after last dose. • Treat- Peak plasma concentration: 4–6 hrs.
ment may impair fertility. • Do not take Protein binding: 91%. Metabolized in
newly prescribed medications unless ap- liver. Excreted in feces (63%) and urine
proved by the prescriber who originally (22%). Half-life: 42 hrs.
started treatment. • Do not ingest
grapefruit products. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Avoid preg-
nancy. May cause fetal harm. Contra-
crizotinib ception should be considered during
therapy and for at least 12 wks after
kriz-o-ti-nib discontinuation. Do not initiate therapy
(Xalkori) until pregnancy status confirmed. Un-
known if crosses placenta or distributed
uCLASSIFICATION in breast milk. Nursing mothers must dis-
PHARMACOTHERAPEUTIC: Tyrosine continue either nursing or drug therapy.
kinase inhibitor. Anaplastic lympho- Children: Safety and efficacy not estab-
ma kinase inhibitor. CLINICAL: Anti- lished. Elderly: No age-related precau-
neoplastic. tions noted.
INTERACTIONS
USES DRUG: Strong CYP3A4 inhibitors
Treatment of locally advanced or meta- (e.g., clarithromycin, ketoconazole,
static non–small-cell lung cancer (NSCLC) ritonavir) may increase concentra-
that is anaplastic lymphoma kinase (ALK) tion/effect. Strong CYP3A4 inducers
positive. Metastatic NSCLC in pts whose tu- (e.g., carBAMazepine, phenytoin, ri-
mors are ROS1 positive. fAMPin) may decrease concentration/ef-
fect. May increase concentration/effect of
PRECAUTIONS aprepitant, bosutinib, budesonide,
Contraindications: Hypersensitivity to cobimetinib, cycloSPORINE, iv-
crizotinib. Cautions: Baseline hepatic abradine, neratinib, sirolimus, ta-
impairment, congenital long QT inter- crolimus. HERBAL: St. John’s wort
val syndrome. Pregnancy (avoid use). may decrease concentration/effect.
Concomitant use of CYP3A4 inducers/ FOOD: Grapefruit products may in-
inhibitors, medications known to cause crease concentration/toxicity (potential
bradycardia, renal impairment. for torsades, myelotoxicity). LAB VAL-
UES: May increase serum ALT, AST, alka-
ACTION line phosphatase, bilirubin. May decrease
Inhibits receptor tyrosine kinases, includ- neutrophils, platelets, lymphocytes.
ing anaplastic lymphoma kinase (ALK),
hepatocyte growth factor receptors AVAILABILITY (Rx)
(HGFR, c-Met), recepteur d’origine nan- Capsules: 200 mg, 250 mg.

Canadian trade name Non-Crushable Drug High Alert drug


280 crizotinib

ADMINISTRATION/HANDLING recovery to Grade 2 or less, then resume


• May give without regard to at 250 mg once daily. Recurrent Grade
food. • Avoid grapefruit prod- 4 toxicity on 250 mg once daily: Per-
C ucts. • Do not break, crush, dissolve, manently discontinue.
or divide capsules. Cardiac
Grade 3 QTc prolongation on at least
INDICATIONS/ROUTES/DOSAGE 2 separate ECGs: Withhold treatment
Non–Small-Cell Lung Cancer (ALK until recovery to baseline or Grade 1 or
Positive), Metastatic NSCLC, ROS-1 less. Resume at 200 mg twice daily. Recur-
Positive rent Grade 3 QTc prolongation on 200
PO: ADULTS: 250 mg twice daily. mg twice daily: Withhold treatment un-
Continue until disease progression or til recovery to baseline or Grade 1 or less.
unacceptable toxicity. Dosage Modifi- Resume at 250 mg once daily. Recurrent
cation: Interrupt and/or reduce to 200 Grade 3 QTc prolongation on 250 mg
mg twice daily based on graded pro- once daily: Permanently discontinue.
tocol, including hematologic toxicity
(Grade 4), elevated LFT with bilirubin Bradycardia
elevation (Grade 1), QT prolongation Grades 2 or 3: Withhold until recovery
(Grade 3). May reduce to 250 mg once to asymptomatic bradycardia or heart
daily if indicated. Discontinue treat- rate 60 or more beats/min, evaluate
ment for QT prolongation (Grade 4), concomitant medications, then resume
elevated LFT with bilirubin elevation at 200 mg twice daily. Grade 4 due to
(Grades 2, 3, 4), pneumonitis of any crizotinib: Permanently discontinue.
grade. Grade 4 associated with concurrent
medications known to cause brady-
cardia/hypotension: Withhold until
Dosage in Renal Impairment
CrCl less than 30 mL/min: 250 mg recovery to asymptomatic bradycardia or
once daily. heart rate 60 or more beats/min, and if
concurrent medications can be stopped,
Dosage in Hepatic Impairment
resume at 250 mg once daily.
No dose adjustment (see dose for hepato- Pulmonary
toxicity during treatment). Pulmonary toxicity: Permanently dis-
continue.
Dose Modification
Hematologic SIDE EFFECTS
Grade 3 toxicity (WBC 1,000–2,000 Frequent (62%–27%): Diplopia, photop-
cells/mm3, ANC 500–1,000 cells/ sia, photophobia, blurry vision, visual
mm3, platelets 25,000–50,000 cells/ field defect, vitreous floaters, reduced
mm3), Grade 3 anemia: Withhold visual acuity, nausea, diarrhea, vomit-
treatment until recovery to Grade 2 or ing, peripheral/localized edema, consti-
less, then resume at same dosage. Grade pation. Occasional (20%–4%): Fatigue,
4 toxicity (WBC less than 1,000 decreased appetite, dizziness, neuropa-
cells/mm3, ANC less than 500 cells/ thy, paresthesia, dysgeusia, dyspepsia,
mm3, platelets less than 25,000 dysphagia, esophageal obstruction/pain/
cells/mm3), Grade 4 anemia: With- spasm/ulcer, odynophagia, reflux esoph-
hold treatment until recovery to Grade agitis, rash, abdominal pain/tenderness,
2 or less, then resume at 200 mg twice stomatitis, glossodynia, glossitis, cheilitis,
daily. Grade 4 toxicity on 200 mg mucosal inflammation, oropharyngeal
twice daily: Withhold treatment until pain/discomfort, bradycardia, headache,

underlined – top prescribed drug


cyclobenzaprine 281
cough. Rare (3%–1%): Musculoskeletal C­ onsider ophthalmological evaluation for
chest pain, insomnia, dyspnea, arthral- vision changes. Reinforce birth control
gia, nasopharyngitis, rhinitis, pharyngi- compliance.
tis, URI, back pain, complex renal cysts, C
PATIENT/FAMILY TEACHING
chest pain/tightness.
• Blood levels will be drawn rou-
ADVERSE EFFECTS/TOXIC tinely. • Report urine changes, bloody
REACTIONS or clay-colored stools, upper abdominal
Severe, sometimes fatal treatment-related pain, nausea, vomiting, bruising, fever,
pneumonitis, pneumonia, dyspnea, pul- cough, difficulty breathing. • Report
monary embolism in less than 2% of history of liver abnormalities or heart
pts was noted. Grade 3–4 elevation of problems, including long QT syndrome,
hepatic enzymes, increased QT prolon- syncope, palpitations, extremity swell-
gation may require discontinuation. May ing. • Immediately report any newly
cause thrombocytopenia, neutropenia, prescribed medications, suspected
lymphopenia. Severe/worsening vitreous pregnancy, or vision changes, including
floaters, photopsia may indicate retinal light flashes, blurred vision, photopho-
hole, retinal detachment. bia, or new or increased float-
ers. • Contraception recommended
NURSING CONSIDERATIONS during treatment and for at least 3 mos
after treatment. • Avoid alcohol,
BASELINE ASSESSMENT
grapefruit products.
Assess vital signs, O2 saturation. Obtain
baseline CBC with differential, serum
chemistries, LFT, PT/INR, ECG. Ques-
tion possibility of pregnancy or plans cyclobenzaprine
for breastfeeding. Obtain full medication
history including vitamins, herbal prod- sye-kloe-ben-za-preen
ucts. Detection of ALK-positive NSCLC test (Amrix, Fexmid)
needed prior to treatment. Assess history Do not confuse cyclobenzaprine
of tuberculosis, HIV, HF, bradyarrhyth- with cycloSERINE or cyprohep-
mias, electrolyte imbalance, medications tadine, or Flexeril with Floxin.
that prolong QT interval. Assess visual
acuity, history of vitreous floaters. Offer uCLASSIFICATION
emotional support. PHARMACOTHERAPEUTIC: Cen-
trally acting muscle relaxant. CLINI-
INTERVENTION/EVALUATION
CAL: Skeletal muscle relaxant.
Assess vital signs, O2 saturation routinely.
Monitor CBC with differential monthly,
LFT, monthly; increase testing for Grades USES
2, 3, 4 adverse effects. Obtain ECG for Treatment of muscle spasm associated
bradycardia, electrolyte imbalance, with acute, painful musculoskeletal con-
chest pain, difficulty breathing. Monitor ditions. OFF-LABEL: Treatment of muscle
for bruising, hematuria, jaundice, right spasms associated with temporomandib-
upper abdominal pain, weight loss, or ular joint pain (TMJ).
acute infection (fever, diaphoresis, leth-
argy, oral mucosal changes, productive PRECAUTIONS
cough). Report decrease in RBC, Hgb, Contraindications:Hypersensitivity to cy-
Hct, platelets, neutrophils, lymphocytes. clobenzaprine. Acute recovery phase of MI,
Worsening cough, fever, or shortness arrhythmias, HF, heart block, conduction
of breath may indicate pneumonitis. disturbances, hyperthyroidism, use within

Canadian trade name Non-Crushable Drug High Alert drug


282 cyclobenzaprine
14 days of MAOIs. Cautions: Hepatic im- ADMINISTRATION/HANDLING
pairment, history of urinary hesitancy or re- PO
tention, angle-closure glaucoma, increased • Give without regard to food. • Do
C intraocular pressure (IOP), elderly. not break, crush, dissolve, or divide ex-
tended-release capsule. • Give ex-
ACTION
tended-release capsule at same time
Centrally acting skeletal muscle relaxant each day.
that reduces tonic somatic muscle activity
at level of brainstem. Influences both al- INDICATIONS/ROUTES/DOSAGE
pha and gamma motor neurons. Thera- b ALERT c Do not use longer than 2–3
peutic Effect: Relieves local skeletal wks.
muscle spasm.
Acute, Painful Musculoskeletal
PHARMACOKINETICS Conditions
Route Onset Peak Duration PO: ADULTS, ELDERLY, CHILDREN 15 YRS
PO 1 hr 3–4 hrs 12–24 hrs AND OLDER: Initially, 5 mg 3 times/day.
May increase to 7.5–10 mg 3 times/day.
Well but slowly absorbed from GI tract. PO: (Extended-Release): ADULTS: 15–
Protein binding: 93%. Metabolized in 30 mg once daily. Not recommended in
GI tract and liver. Primarily excreted in elderly.
urine. Half-life: 8–37 hrs.
Dosage in Renal Impairment
LIFESPAN CONSIDERATIONS No dose adjustment.
Pregnancy/Lactation: Unknown if
drug crosses placenta or is distributed Dosage in Hepatic Impairment
in breast milk. Children: Safety and effi- Note: Extended-release capsule not rec-
cacy not established. Elderly: Increased ommended in hepatic impairment. Mild
sensitivity to anticholinergic effects (e.g., impairment: 5 mg 3 times/day. Mod-
confusion, urinary retention). Increased erate to severe impairment: Not rec-
risk of falls, fractures. Not recommended. ommended.

INTERACTIONS SIDE EFFECTS


DRUG: Alcohol, other CNS depres- Frequent (39%–11%): Drowsiness, dry
sant medications (e.g., lorazepam, mouth, dizziness. Rare (3%–1%): Fatigue,
morphine, zolpidem) may increase asthenia, blurred vision, headache, anxi-
CNS depression. MAOIs (e.g., phenel- ety, confusion, nausea, constipation, dys-
zine, selegiline) may increase risk of pepsia, unpleasant taste.
hypertensive crisis, seizures. Anticho-
linergics (e.g., aclidinium, ipratro- ADVERSE EFFECTS/TOXIC
pium, umeclidinium) may increase REACTIONS
anticholinergic effect. HERBAL: Herb- Overdose may result in visual hallucina-
als with sedative properties (e.g., tions, hyperactive reflexes, muscle rigid-
chamomile, kava kava, valerian) may ity, vomiting, hyperpyrexia.
increase CNS depression. FOOD: None
known. LAB VALUES: None significant. NURSING CONSIDERATIONS
AVAILABILITY (Rx) BASELINE ASSESSMENT
Tablets: 5 mg, 7.5 mg, 10 mg. Suspen- Record onset, type, location, duration of
sion, Oral: 1 mg/mL. muscular spasm. Check for immobility,
stiffness, swelling.
Capsules: (Extended-Release [Am-
rix]): 15 mg, 30 mg.
underlined – top prescribed drug
cyclophosphamide 283
INTERVENTION/EVALUATION PRECAUTIONS
Assist with ambulation. Assess for thera- Contraindications: Hypersensitivity to
peutic response: relief of pain; decreased cyclophosphamide. Urinary outflow ob-
stiffness, swelling; increased joint mobil- struction. Cautions: Severe leukopenia, C
ity; reduced joint tenderness; improved thrombocytopenia, tumor infiltration of
grip strength. bone marrow, previous therapy with other
PATIENT/FAMILY TEACHING antineoplastic agents, radiation, renal/he-
patic/cardiac impairment, active UTI.
• Avoid tasks that require alertness,
­motor skills until response to drug is es- ACTION
tablished. • Drowsiness usually dimin- Inhibits DNA, RNA protein synthesis by
ishes with continued therapy. • Avoid cross-linking with DNA, RNA strands. Cell
alcohol, other depressants while taking cycle–phase nonspecific. Therapeutic
medication. • Avoid sudden changes in Effect: Prevents cell growth. Potent im-
posture. • Sugarless gum, sips of water munosuppressant.
may relieve dry mouth.
PHARMACOKINETICS
Well absorbed from GI tract. Protein
binding: 10%–60%. Crosses blood-brain
cyclophosphamide barrier. Metabolized in liver. Primarily
excreted in urine. Removed by hemodi-
sye-kloe-foss-fa-mide alysis. Half-life: 3–12 hrs.
(Procytox )
Do not confuse cyclophospha-
mide with cycloSPORINE or
LIFESPAN CONSIDERATIONS
ifosfamide. Pregnancy/Lactation: If possible, avoid
use during pregnancy. Use of effective
uCLASSIFICATION contraception during therapy and up to
PHARMACOTHERAPEUTIC: Alkylat- 1 yr after completion of therapy is recom-
ing agent. CLINICAL: Antineoplastic. mended. May cause fetal malformations
(limb abnormalities, cardiac anomalies,
hernias). Distributed in breast milk.
USES Breastfeeding not recommended. Chil-
Treatment of acute lymphocytic, acute dren: No age-related precautions noted.
nonlymphocytic, chronic myelocytic, Elderly: Age-related renal impairment
chronic lymphocytic leukemias; ovarian, may require dosage adjustment.
breast carcinomas; neuroblastoma; reti-
noblastoma; Hodgkin’s, non-Hodgkin’s INTERACTIONS
lymphomas; multiple myeloma; mycosis DRUG: CYP2D6 inducers (e.g., car-
fungoides; nephrotic syndrome in chil- BAMazepine, PHENobarbital) may de-
dren. OFF-LABEL: Treatment of adreno- crease concentration/effect. Anthracycline
cortical, bladder, cervical, endometrial, agents (e.g., DOXOrubicin, epiRUBi-
prostatic, testicular carcinomas; Ewing’s cin) may increase risk of cardiomyopathy.
sarcoma; multiple sclerosis; non–small- Live virus vaccines may potentiate virus
cell, small-cell lung cancer; organ trans- replication, increase vaccine side effects,
plant rejection; osteosarcoma; ovarian decrease pt’s antibody response to vaccine.
germ cell, primary brain, trophoblastic HERBAL: Pts with an estrogen-dependent
tumors; rheumatoid arthritis; soft-tissue tumor should avoid black cohosh, dong
sarcomas; systemic dermatomyositis; sys- quai. FOOD: None known. LAB VAL-
temic lupus erythematosus; Wilms’ tumor. UES: May increase serum uric acid.

Canadian trade name Non-Crushable Drug High Alert drug


284 cyclophosphamide

AVAILABILITY (Rx) PO: ADULTS, ELDERLY, CHILDREN: 1–5


mg/kg/day.
Capsules: 25 mg, 50 mg. Injection,
C Powder for Reconstitution: 500 mg, 1 g, Nephrotic Syndrome
2 g. PO: ADULTS, CHILDREN: 2 mg/kg/day
for 60–90 days. Maximum cumulative
ADMINISTRATION/HANDLING dose: 168 mg/kg.
b ALERT c May be carcinogenic, muta-
genic, teratogenic. Handle with extreme Dosage in Renal/Hepatic Impairment
care during preparation/administration. No dose adjustment. Use caution.
IV SIDE EFFECTS
Reconstitution • Reconstitute each Expected: Marked leukopenia 8–15
100 mg with 5 mL Sterile Water for Injec- days after initiation. Frequent: Nausea,
tion, 0.9% NaCl, or D5W to provide con- vomiting (beginning about 6 hrs after
centration of 20 mg/mL. • Shake to administration and lasting about 4 hrs);
dissolve. • Allow to stand until clear. alopecia (33%). Occasional: Diarrhea,
Rate of administration • Infusion darkening of skin/fingernails, stomatitis,
rates vary based on protocol. May give by headache, diaphoresis. Rare: Pain/red-
direct IV injection, IV piggyback, or con- ness at injection site.
tinuous IV infusion.
Storage • Reconstituted solution in ADVERSE EFFECTS/TOXIC
0.9% NaCl is stable for 24 hrs at room REACTIONS
temperature or up to 6 days if refriger- Myelosuppression resulting in blood
ated. dyscrasias (leukopenia, anemia,
thrombocytopenia, hypoprothrombin-
PO emia) has been noted. Expect leukope-
• Give on an empty stomach. If GI upset nia to resolve in 17–28 days. Anemia
occurs, give with food. • Do not cut or generally occurs after large doses or
crush. • To minimize risk of bladder prolonged therapy. Thrombocytope-
irritation, do not give at bedtime. nia may occur 10–15 days after drug
initiation. Hemorrhagic cystitis oc-
IV INCOMPATIBILITIES curs commonly in long-term therapy
Amphotericin B complex (Abelcet, AmBi- (esp. in children). Pulmonary fibrosis,
some, Amphotec). cardiotoxicity noted with high doses.
Amenorrhea, azoospermia, hyperkale-
IV COMPATIBILITIES mia may occur.
Granisetron (Kytril), heparin, HYDRO-
morphone (Dilaudid), LORazepam (Ati- NURSING CONSIDERATIONS
van), morphine, ondansetron (Zofran), BASELINE ASSESSMENT
propofol (Diprivan).
Obtain CBC wkly during therapy or until
INDICATIONS/ROUTES/DOSAGE maintenance dose is established, then
Note: Hematologic toxicity may require at 2- to 3-wk intervals. Question his-
dose reduction. tory of urinary outlet flow obstruction,
hepatic/renal impairment, active infec-
Usual Dosage (Refer to Individual tions. Obtain urine/serum pregnancy
Protocols) test.
IV: ADULTS, ELDERLY, CHILDREN:(Single INTERVENTION/EVALUATION
agent): 40–50 mg/kg in divided doses
over 2–5 days or 10–15 mg/kg q7–10 Monitor CBC, serum BUN, creatinine,
days or 3–5 mg/kg twice wkly. electrolytes, urine output. Monitor WBC

underlined – top prescribed drug


cycloSPORINE 285
counts closely during initial therapy. uCLASSIFICATION
Monitor for hematologic toxicity (fever, PHARMACOTHERAPEUTIC: Cal-
sore throat, signs of local infection, un- cineurin inhibitor. CLINICAL: Immu-
usual bruising/bleeding from any site), nosuppressant. C
symptoms of anemia (excessive fatigue,
weakness). Recovery from marked leu-
kopenia due to myelosuppression can be USES
expected in 17–28 days.
Modified, Nonmodified: Prevents or-
PATIENT/FAMILY TEACHING gan rejection of kidney, liver, heart in
• Encourage copious fluid intake, fre- combination with steroid therapy and
quent voiding (assists in preventing cysti- an antiproliferative immunosuppres-
tis) at least 24 hrs before, during, after sive agent. Nonmodified: Treatment
therapy. • Do not have immunizations of chronic allograft rejection in those
without physician’s approval (drug low- previously treated with other immu-
ers resistance). • Avoid contact with nosuppressives. Modified: Treatment
those who have recently received live vi- of severe, active rheumatoid arthritis,
rus vaccine. • Promptly report fever, severe recalcitrant plaque psoriasis in
sore throat, signs of local infection, dif- nonimmunocompromised adults. Oph-
ficulty or pain with urination, unusual thalmic: Chronic dry eyes. OFF-LABEL:
bruising/bleeding from any site. • Hair Allogenic stem cell transplants for
loss is reversible, but new hair growth prevention/treatment of graft-vs-host
may have different color, tex- disease; focal segmental glomeruloscle-
ture. • Avoid pregnancy for up to 1 yr rosis, lupus nephritis, severe ulcerative
after completion of treatment. colitis.
PRECAUTIONS
Contraindications: History of hypersensi-
cycloSPORINE tivity to cycloSPORINE, polyoxyethylated
castor oil; rheumatoid arthritis, psoria-
sye-kloe-spor-in sis, uncontrolled hypertension, renal im-
(Gengraf, Neoral, Restasis, SandIM- pairment, or malignancies in treatment
MUNE) of psoriasis or rheumatoid arthritis. Cau-
j BLACK BOX ALERT j Only tions: Hepatic/renal impairment. History
physicians experienced in manage- of seizures. Avoid live vaccines.
ment of immunosuppressive therapy
and organ transplant pts should ACTION
prescribe. Renal impairment may oc-
cur with high dosage. Increased risk Inhibits cellular, humoral immune re-
of neoplasia, susceptibility to infec- sponses by inhibiting interleukin-2, a
tions. May cause hypertension, ne- proliferative factor needed for T-cell
phrotoxicity. Psoriasis pts: Increased activity. Therapeutic Effect: Prevents
risk of developing skin malignan- organ rejection, relieves symptoms of
cies. The modified/nonmodified
formulations are not bioequivalent psoriasis, arthritis.
and cannot be used interchangeably
without close monitoring. PHARMACOKINETICS
Do not confuse cycloSPORINE Variably absorbed from GI tract. Pro-
with cycloSERINE or cyclophos- tein binding: 90%. Metabolized in liver.
phamide, Gengraf with ProGraf, Eliminated primarily by biliary or fecal
Neoral with Neurontin or excretion. Not removed by hemodialysis.
Nizoral, or SandIMMUNE with Half-life: Adults, 10–27 hrs; children,
SandoSTATIN. 7–19 hrs.

Canadian trade name Non-Crushable Drug High Alert drug


286 cycloSPORINE

LIFESPAN CONSIDERATIONS IV
Pregnancy/Lactation: Readily crosses
placenta. Distributed in breast milk. Reconstitution • Dilute each mL (50
C mg) concentrate with 20–100 mL 0.9%
Breastfeeding not recommended. Chil-
dren: No age-related precautions noted
NaCl or D5W (maximum concentra-
in transplant pts. Elderly: Increased tion: 2.5 mg/mL).
Rate of administration • Infuse over
risk of hypertension, increased serum
creatinine. 2–6 hrs. • Monitor pt continuously for
hypersensitivity reaction (facial flushing,
INTERACTIONS dyspnea).
Storage • Store parenteral form at
DRUG: May increase concentration/
effects of aliskiren, atorvastatin, room temperature. • Protect IV solution
dronedarone, lovastatin, pazo- from light. • After diluted, stable for 6
panib, simvastatin. Strong CYP3A4 hrs in PVC; 24 hrs in non-PVC or glass.
inhibitors (e.g., clarithromycin, ke- PO
toconazole, ritonavir) may increase • Administer consistently with relation
concentration/effect. Strong CYP3A4 to time of day and meals. • Oral solu-
inducers (e.g., carBAMazepine, tion may be mixed in glass container with
phenytoin, rifAMPin) may decrease milk, chocolate milk, orange juice, or
concentration/effect. Live virus vac- apple juice (preferably at room tempera-
cines may potentiate virus replication, ture). Stir well. • Drink immedi-
increase vaccine side effects, decrease ately. • Add more diluent to glass con-
pt’s response to vaccine. HERBAL: Echi- tainer. Mix with remaining solution to
nacea may decrease therapeutic ef- ensure total amount is given. • Dry
fect. FOOD: Grapefruit products may outside of calibrated liquid measuring
increase absorption/immunosuppres- device before replacing cover. • Do not
sion, risk of toxicity. LAB VALUES: May rinse with water. • Avoid refrigeration
increase serum BUN, alkaline phos- of oral solution (solution may sepa-
phatase, amylase, bilirubin, creatinine, rate). • Discard oral solution after 2
potassium, uric acid, ALT, AST. May de- mos once bottle is opened.
crease serum magnesium. Therapeutic
peak serum level: 50–400 ng/mL; Ophthalmic
toxic serum level: greater than 400 • Invert vial several times to obtain uni-
ng/mL. form suspension. • Instruct pt to remove
AVAILABILITY (Rx) contact lenses before administration (may
reinsert 15 min after administra-
Capsules: (Gengraf, Neoral [Modi- tion). • May use with artificial tears.
fied], SandIMMUNE [Nonmodified]): 25
mg, 50 mg, 100 mg. Injection, Solution: IV INCOMPATIBILITIES
(SandIMMUNE): 50 mg/mL. Ophthalmic Acyclovir (Zovirax), amphotericin B
Emulsion: (Restasis): 0.05%. Oral Solu- complex (Abelcet, AmBisome, Ampho-
tion: (Gengraf, Neoral [Modified], SandIM- tec), magnesium.
MUNE [Nonmodified]): 100 mg/mL.
IV COMPATIBILITIES
ADMINISTRATION/HANDLING
Propofol (Diprivan).
b ALERT c Oral solution available in
bottle form with calibrated liquid mea- INDICATIONS/ROUTES/DOSAGE
suring device. Oral form should re- Note: The modified/nonmodified for-
place IV administration as soon as mulations are not bioequivalent and
possible. cannot be used interchangeably without

underlined – top prescribed drug


cycloSPORINE 287
close monitoring. Refer to institutional (4%–2%): Acne, leg cramps, gingival hy-
protocols. Dosing in clinical practice perplasia (red, bleeding, tender gums),
may differ greatly compared to manufac- paresthesia, diarrhea, nausea, vomiting,
turer’s labeling. headache. Rare (less than 1%): Hypersen- C
sitivity reaction, abdominal discomfort,
Transplantation, Prevention of Organ gynecomastia, sinusitis.
Rejection
Note: Initial dose given 4–12 hrs prior ADVERSE EFFECTS/TOXIC
to transplant or postoperatively. REACTIONS
PO: ADULTS, ELDERLY, CHILDREN: Not Mild nephrotoxicity occurs in 25% of renal
modified: Initially, 10–12 mg/kg daily transplants, 38% of cardiac transplants,
for 1–2 wks, then taper by 5% each wk to 37% of liver transplants, generally 2–3 mos
maintenance dose of 5–10 mg/kg daily. after transplantation (more severe toxic-
Modified: (dose dependent upon type ity may occur soon after transplantation).
of transplant). Renal: 6–12 mg/kg/day Hepatotoxicity occurs in 4% of renal, 7%
in 2 divided doses. Hepatic: 4–12 mg/kg/ of cardiac, and 4% of liver transplants, gen-
day in 2 divided doses. Heart: 4–10 mg/ erally within first mo after transplantation.
kg/day in 2 divided doses. Both toxicities usually respond to dosage
IV: ADULTS, ELDERLY, CHILDREN: Not reduction. Severe hyperkalemia, hyperuri-
modified: Initially, 5–6 mg/kg/dose cemia occur occasionally.
daily. Switch to oral as soon as possible.
NURSING CONSIDERATIONS
Rheumatoid Arthritis
PO: ADULTS, ELDERLY: Modified: Ini- BASELINE ASSESSMENT
tially, 2.5 mg/kg a day in 2 divided doses. Obtain baseline serum chemistries, esp.
May increase by 0.5–0.75 mg/kg/day af- renal function, LFT. If nephrotoxicity oc-
ter 8 wks with additional increases made curs, mild toxicity is generally noted 2–3
at 12 wks. Maximum: 4 mg/kg/day. mos after transplantation; more severe
toxicity noted early after transplantation;
Psoriasis hepatotoxicity may be noted during first
PO: ADULTS, ELDERLY: Modified: Ini- mo after transplantation.
tially, 2.5 mg/kg/day in 2 divided doses.
May increase by 0.5 mg/kg/day after 4 INTERVENTION/EVALUATION
wks; additional increases may be made Diligently monitor serum BUN, creati-
q2wks. Maximum: 4 mg/kg/day. nine, bilirubin, ALT, AST, LDH levels for
evidence of hepatotoxicity/nephrotoxic-
Dry Eye
ity (mild toxicity noted by slow rise in
Ophthalmic: ADULTS, ELDERLY: Instill 1 serum levels; more overt toxicity noted
drop in each affected eye q12h. by rapid rise in levels; hematuria also
Dosage in Renal Impairment noted in nephrotoxicity). Monitor se-
Modify dose if serum creatinine levels rum potassium for evidence of hyperka-
25% or above pretreatment levels. lemia. Encourage diligent oral hygiene
(gingival hyperplasia). Monitor B/P for
Dosage in Hepatic Impairment evidence of hypertension. Note: Refer-
Mild to moderate impairment: No ence ranges dependent on organ trans-
dose adjustment. Severe impair- planted, organ function, cycloSPORINE
ment: Use caution. toxicity. Trough levels should be ob-
tained immediately prior to next dose.
SIDE EFFECTS Therapeutic serum level: 50–400
Frequent (26%–12%): Mild to moderate hy- ng/mL; toxic serum level: greater than
pertension, hirsutism, tremor. Occasional 400 ng/mL.

Canadian trade name Non-Crushable Drug High Alert drug


288 cytarabine
PATIENT/FAMILY TEACHING geal infection. Cautions: Renal/hepatic
• Blood levels will be drawn rou- impairment, prior drug-induced bone
tinely. • Report severe headache, marrow suppression.
C persistent nausea /vomiting, unusual
­
swelling of extremities, chest ACTION
pain. • Avoid grapefruit products (in- Inhibits DNA polymerase. Cell cycle–spe-
creases concentration/effects), St. cific for S phase of cell division. Thera-
John’s wort (decreases concentra- peutic Effect: Inhibits DNA synthesis.
tion). • Do not take any newly pre- Potent immunosuppressive activity.
scribed or OTC medications unless ap-
proved by the prescriber who originally PHARMACOKINETICS
started treatment. Widely distributed; moderate amount
crosses blood-brain barrier. Protein
binding: 15%. Primarily excreted in
cytarabine urine. Half-life: 1–3 hrs.
LIFESPAN CONSIDERATIONS
sye-tar-a-bine
(Ara-C, Cytosar-U , Depo-Cyt ) Pregnancy/Lactation: If possible,
avoid use during pregnancy. May cause
j BLACK BOX ALERT j Must be fetal malformations. Unknown if dis-
administered by personnel trained
in administration/handling of chem- tributed in breast milk. Breastfeeding
otherapeutic agents. Conventional: not recommended. Children: No age-
Potent myelosuppressant. High related precautions noted. Elderly: Age-
risk of multiple toxicities (GI, CNS, related renal impairment may require
pulmonary, cardiac). Liposomal:
Chemical arachnoiditis, manifested dosage adjustment.
by profound nausea, vomiting,
fever, may be fatal if untreated. INTERACTIONS
Do not confuse cytarabine with DRUG: May decrease therapeutic ef-
Cytoxan or vidarabine, or Cyto- fect of BCG (intravesical), vaccines
sar with Cytoxan or Neosar. (live). May increase adverse effects of
vaccines (live). May increase adverse
uCLASSIFICATION effects of natalizumab. HERBAL: Echi-
PHARMACOTHERAPEUTIC: Antime- nacea may decrease therapeutic effect.
tabolite. CLINICAL: Antineoplastic. FOOD: None known. LAB VALUES: May
increase serum alkaline phosphatase,
bilirubin, uric acid, AST.
USES
Conventional: Remission induction in AVAILABILITY (Rx)
acute myeloid leukemia (AML), treat- Injection, Powder for Reconstitution (Con-
ment of acute lymphocytic leukemia ventional): 100 mg, 500 mg, 1 g. Injec-
(ALL) and chronic myelocytic leuke- tion, Solution (Conventional): 20 mg/mL,
mia (CML), prophylaxis and treatment 100 mg/mL. Injection, Suspension (Lipo-
of meningeal leukemia. Liposomal: somal): 10 mg/mL.
Treatment of lymphomatous meningitis.
OFF-LABEL: Ara-C: Carcinomatous men- ADMINISTRATION/HANDLING
ingitis, Hodgkin’s and non-Hodgkin’s b ALERT c May give by subcutaneous,
lymphomas, myelodysplastic syndrome. IV push, IV infusion, intrathecal routes at
concentration not to exceed 100 mg/mL.
PRECAUTIONS May be carcinogenic, mutagenic, terato-
Hypersensitivity to
Contraindications: genic (embryonic deformity). Handle
cytarabine. Liposomal: Active menin- with extreme care during preparation/
underlined – top prescribed drug
cytarabine 289
administration. Liposomal for intrathecal SIDE EFFECTS
use only. Frequent: IV (33%–16%): Asthenia,
fever, pain, altered taste/smell, nausea,
IV, Intrathecal C
vomiting (risk greater with IV push than
Reconstitution • Conventional: with continuous IV infusion). Intrathe-
Reconstitute with Bacteriostatic Water for cal (28%–11%): Headache, asthenia,
Injection. • Dose may be further altered taste/smell, confusion, drowsi-
diluted with 250–1,000 mL D5W or 0.9% ness, nausea, vomiting. Occasional: IV
NaCl for IV infusion. • Intrathecal: (11%–7%): Abnormal gait, drowsiness,
reconstitute vial with preservative-free constipation, back pain, urinary inconti-
0.9% NaCl or pt’s spinal fluid. Dose nence, peripheral edema, headache,
usually administered in 5–15 mL of confusion. Intrathecal (7%–3%): Pe-
solution, after equivalent volume of CSF ripheral edema, back pain, constipation,
removed. • Liposomal: No reconstitu­ abnormal gait, urinary incontinence.
tion required.
Rate of administration • Conven- ADVERSE EFFECTS/ TOXIC
tional: For IV infusion, give over 1–3 hrs REACTIONS
or as continuous infusion.
Myelosuppression resulting in blood
Storage • Conventional: Store at room
dyscrasias (leukopenia, anemia, throm-
temperature. • Reconstituted solution
bocytopenia, megaloblastosis, reticulo-
is stable for 48 hrs at room tempera-
cytopenia), occurring minimally after
ture. • Use diluted solution within 24
single IV dose. Leukopenia, anemia,
hrs. • Discard if slight haze devel-
thrombocytopenia should be expected
ops. • Liposomal: Refrigerate; use within
with daily or continuous IV therapy. Cy-
4 hrs following withdrawal from vial.
tarabine syndrome (fever, myalgia, rash,
IV INCOMPATIBILITIES conjunctivitis, malaise, chest pain),
hyperuricemia may occur. High-dose
Amphotericin B complex (Abelcet, Am- therapy may produce severe CNS, GI,
Bisome, Amphotec), ganciclovir (Cyto- pulmonary toxicity.
vene), heparin, insulin (regular).
NURSING CONSIDERATIONS
IV COMPATIBILITIES
Dexamethasone (Decadron), diphen- BASELINE ASSESSMENT
hydrAMINE (Benadryl), filgrastim Obtain baseline CBC, renal function, LFT.
(Neupogen), granisetron (Kytril), HY- Leukocyte count decreases within 24 hrs
DROmorphone (Dilaudid), LORazepam after initial dose, continues to decrease
(Ativan), morphine, ondansetron (Zo- for 7–9 days followed by brief rise at 12
fran), potassium chloride, propofol (Di- days, decreases again at 15–24 days, then
privan). rises rapidly for next 10 days. Platelet
count decreases 5 days after drug ini-
INDICATIONS/ROUTES/DOSAGE tiation to its lowest count at 12–15 days,
Usual Dosage for Induction (Conventional) then rises rapidly for next 10 days.
(Refer to Individual Protocols)
INTERVENTION/EVALUATION
IV: ADULTS, ELDERLY, CHILDREN: (Induc-
tion):100 mg/m2/day continuous infu- Monitor BMP, LFT; serum uric acid.
sion for 7 days or 200 mg/m2/day con- Monitor CBC for evidence of my-
tinuous infusion (as 100 mg/m2 over 12 elosuppression. Monitor for blood
hrs q12h) for 7 days. dyscrasias (fever, sore throat, signs
of local infection, unusual bruising/
Dosage in Renal/Hepatic Impairment bleeding from any site), symptoms of
No dose adjustment. anemia (excessive fatigue, weakness).

Canadian trade name Non-Crushable Drug High Alert drug


290 cytarabine
Monitor for signs of neuropathy (gait immunizations without physician’s ap-
disturbances, handwriting difficulties, proval (drug lowers resistance). • Avoid
paresthesia). contact with those who have recently re-
C ceived live virus vaccine. • Promptly
PATIENT/FAMILY TEACHING
report fever, sore throat, signs of local
• Increase fluid intake (may protect infection, unusual bruising/bleeding
against hyperuricemia). • Do not have from any site.

underlined – top prescribed drug


dabigatran 291
LIFESPAN CONSIDERATIONS
dabigatran Pregnancy/Lactation: Unknown if dis-
tributed in breast milk. Children: Safety
dab-i-gah-tran and efficacy not established in pts
(Pradaxa) younger than 18 yrs. Elderly: Severe
j BLACK BOX ALERT jRisk of renal impairment may require dosage D
thrombotic events (e.g., stroke)
increased if discontinued for a adjustment.
reason other than pathological
bleeding. Spinal or epidural he- INTERACTIONS
matoma may occur with neuraxial DRUG: Amiodarone, dronedarone,
anesthesia. P-glycoprotein/ABCB1 inhibitors (e.g.,
uCLASSIFICATION amiodarone, colchicine, omeprazole)
may increase concentration/effect. Ant-
PHARMACOTHERAPEUTIC: Direct acids, P-glycoprotein (P-gp)/ABCB1
thrombin inhibitor. CLINICAL: Anti- inducers (e.g., carBAMazepine, phe-
coagulant. nytoin) may decrease concentration/
effect. Apixaban, edoxaban may increase
USES anticoagulant effect. Aspirin, vorapaxar
may increase adverse effects. HERBAL:
Indicated to reduce risk of stroke, sys- Herbs with anticoagulant/antiplatelet
temic embolism in pts with nonvalvular properties (e.g., garlic, ginger, ginkgo
atrial fibrillation. Treatment and reduction biloba) may increase effect. St. John’s
of risk of deep vein thrombosis (DVT) and wort may decrease concentration/effect.
pulmonary embolism (PE). Prophylaxis of FOOD: High-fat meal delays absorption
DVT and PE in pts who have undergone approx. 2 hrs. LAB VALUES: May increase
hip replacement surgery. aPTT, PT, INR.
PRECAUTIONS AVAILABILITY (Rx)
Contraindications: Severe hypersensitivity
to dabigatran. Active major bleeding, pts Capsules: 75 mg, 110 mg, 150 mg.
with mechanical prosthetic heart valves. ADMINISTRATION/HANDLING
Cautions: Renal impairment (CrCl 15–30
mL/min), moderate hepatic impairment, PO
invasive procedures, spinal anesthesia, • May be given without regard to food.
major surgery, pts with congenital or Administer with water. • Do not break,
acquired bleeding disorders, elderly, con- cut, open capsules.
current use of medications that increase INDICATIONS/ROUTES/DOSAGE
risk of bleeding, valvular heart disease.
b ALERT c Medication should be dis-
ACTION continued prior to invasive or surgical
Reversible direct thrombin inhibitor procedures.
that inhibits both free and fibrin-bound Treatment/Prevention of DVT/PE
thrombin. Therapeutic Effect: Pro- PO: ADULTS, ELDERLY: 150 mg twice
duces anticoagulation, preventing devel- daily (after 5–10 days of treatment with
opment of thrombus. parenteral anticoagulants).
PHARMACOKINETICS Nonvalvular Atrial Fibrillation
Metabolized in liver. Protein binding: PO: ADULTS, ELDERLY: 150 mg twice
35%. Eliminated primarily in urine. daily (to reduce risk of stroke/systemic
Half-life: 12–17 hrs. embolism).

Canadian trade name Non-Crushable Drug High Alert drug


292 dabrafenib
Prophylaxis Following Hip Surgery surgery; hepatic, renal impairment; recent
PO: ADULTS, ELDERLY: 110 mg on day spinal, epidural procedures; recent hem-
one (1–4 hr postoperative and estab- orrhagic events (intracranial hemorrhage,
lished hemostasis), then 220 mg daily for hemorrhagic stroke, GI/GU bleeding).
up to 35 days. Receive full medication history and screen
D for interactions. Screen for active bleeding.
Dosage in Renal Impairment
Nonvalvular atrial fibrillation: CrCl INTERVENTION/EVALUATION
15–30 mL/min: Reduce dose to 75 Obtain aPTT, platelet count if bleeding
mg twice daily. CrCl less than 15 mL/ occurs. Assess for any signs of bleed-
min, or HD: Not recommended (HD ing (hematuria, melena, bleeding from
removes ∼60% over 2–3 hrs). CrCl gums, petechiae, bruising), hematoma,
30–50 mL/min with concomitant hypotension, tachycardia, abdominal
use of P-gp inhibitors: Reduce dose pain. Question for increase in discharge
to 75 mg twice daily if given with P-gp during menses. Use care when removing
inhibitors dronedarone or ketoconazole adhesives, tape. Monitor for symptoms of
(systemic). CrCl less than 30 mL/min intracranial hemorrhage (altered mental
with concomitant use of P-gp inhibi- status, aphasia, lethargy, hemiparesis,
tors: Avoid coadministration. hemiplegia, seizures, vision changes).
Treatment/Prevention of DVT/PE:
CrCl less than or equal to 30 mL/ PATIENT/FAMILY TEACHING
min: Not specified. CrCl less than 50 • Treatment may increase risk of bleed-
mL/min with concomitant use of P-gp ing. • Report dark or bloody urine,
inhibitors: Avoid coadministration. black or bloody stool, coffee-ground vomi-
Prophylaxis following hip surgery: tus, bloody sputum, nosebleeds. • Stroke-
CrCl less than or equal to 30 mL/ like symptoms may indicate bleeding into
min: Not specified. CrCl less than 50 the brain; report difficulty speaking, head-
mL/min with concomitant use of P-gp ache, numbness, paralysis, vision changes,
inhibitors: Avoid coadministration. seizures. • Do not chew, crush, open, or
divide capsules. • Use electric razor, soft
Dosage in Hepatic Impairment toothbrush to prevent bleeding. • Do not
No dosage adjustment. take newly prescribed medications, includ-
ing OTC medications such as ibuprofen or
SIDE EFFECTS naproxen, unless approved by physician
Frequent (less than 16%):Dyspepsia (heart­ who originally started treatment. • Stop-
burn, nausea, indigestion), diarrhea, upper ping therapy may increase the risk of blood
abdominal pain. clots or stroke.
ADVERSE EFFECTS/TOXIC
REACTIONS
Severe, sometimes fatal, hemorrhagic events, dabrafenib
including intracranial hemorrhage, hemor-
rhagic stroke, Gl bleeding, may occur. Hyper- da-braf-e-nib
sensitivity reactions, including anaphylaxis, (Tafinlar)
reported in less than 1% of pts. Do not confuse dabrafenib with
dasatinib.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT uCLASSIFICATION

Obtain CBC (esp. platelet count), BUN, PHARMACOTHERAPEUTIC: BRAF


serum creatinine; GFR, CrCl. Question kinase inhibitor. CLINICAL: Antineo-
history of mechanical heart valve, ­recent plastic.

underlined – top prescribed drug


dabrafenib 293

USES fertility in females and males. Chil-


Treatment of unresectable or metastatic dren: Safety and efficacy not estab-
melanoma with BRAF V600E mutation lished. Elderly: May have increased risk
(single-agent therapy) or in pts with of adverse effects, skin lesions.
BRAF V600E or V600K mutations (in INTERACTIONS
combination with trametinib). Adjuvant D
treatment of melanoma (in combina- DRUG: Strong CYP2C8 inhibitors
tion with trametinib) in pts with a BRAF (e.g., gemfibrozil), strong CYP3A4
V600E or BRAF V600K mutation, and inhibitors (e.g., clarithromycin,
lymph node involvement. Treatment of ketoconazole, ritonavir) may increase
metastatic non–small-cell lung cancer concentration/effect. Strong CYP3A4
(NSCLC) in pts with BRAF V600E muta- inducers (e.g., carBAMazepine,
tion. Treatment of locally advanced or phenytoin, rifAMPin) may decrease
metastatic anaplastic thyroid cancer (in concentration/effect. May increase con-
combination with trametinib) in pts with centration/effects of pazopanib, topo-
BRAF V600E mutation and with no satis- tecan, voxilaprevir. May decrease
factory locoregional treatment options. concentration/effect of abemaciclib,
axitinib, neratinib, olaparib, rano-
b ALERT c Not indicated for treatment lazine. May decrease effectiveness of
of wild-type BRAF melanomas, wild-type hormonal contraceptives. HERBAL: St.
BRAF NSCLC, or wild-type BRAF anaplas- John’s wort may decrease concentra-
tic thyroid cancer. tion/effect. FOOD: High-fat meals may
PRECAUTIONS decrease absorption/effect. LAB VAL-
UES: May increase serum glucose, alka-
Contraindications: Hypersensitivity to line phosphatase. May decrease serum
dab­rafenib. Cautions: Diabetes, hepatic/ phosphate, sodium.
renal impairment, dehydration, glucose-
6-phosphate dehydrogenase (G6PD) AVAILABILITY (Rx)
deficiency, pts at increased risk for
Capsules: 50 mg, 75 mg.
arrhythmias, HF.
ADMINISTRATION/HANDLING
ACTION
PO
Selectively inhibits some mutant forms of • Give at least 1 hr before or at least 2
protein kinase B-raf (BRAF). Therapeu- hrs after meal. • Do not break, crush,
tic Effect: Inhibits tumor cell growth open, or divide capsule. • Missed dose
and metastasis. may be given up to 6 hrs before next dose.
PHARMACOKINETICS INDICATIONS/ROUTES/DOSAGE
Widely distributed. Metabolized in liver. Melanoma, NSCLC, Thyroid Cancer
Protein binding: 99.7%. Peak plasma PO: ADULTS, ELDERLY: 150 mg twice
concentration: 2 hrs. Excreted in feces daily (about 12 hrs apart). Continue until
(71%), urine (23%). Half-life: 8 hrs. disease progression or unacceptable
toxicity.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Avoid preg- Dose Modification
nancy; may cause fetal harm. Must Based on Common Terminology Criteria
use effective nonhormonal contracep- for Adverse Events (CTCAE).
tion during treatment and for at least 2 Reduction Levels Dose
wks after discontinuation (intrauterine
1st dose reduction 100 mg twice daily
device, barrier methods). Unknown if 2nd dose reduction 75 mg twice daily
distributed in breast milk. May impair 3rd dose reduction 50 mg twice daily

Canadian trade name Non-Crushable Drug High Alert drug


294 dabrafenib
Cardiac of any Grade 4 toxicity: Permanently
Symptomatic HF; absolute decrease in discontinue.
LVEF greater than 20% from baseline
that is below the lower limit of nor- Dosage in Renal Impairment
mal: Withhold treatment until cardiac func- Mild to moderate impairment: No dos-
D tion improves, then resume at same dose. age adjustment. Severe impairment: Not
specified; use caution.
Febrile Drug Reaction
Fever 101.3°F–104°F: Withhold treat- Dosage in Hepatic Impairment
ment until resolved. Then, resume at Mild impairment: No dosage adjust-
same dose (or at reduced dose level). ment. Moderate to severe impairment:
Fever greater than 104°F; fever Not specified; use caution.
associated with dehydration, hypo-
tension, renal failure: Withhold SIDE EFFECTS
treatment until resolved, then resume Frequent (37%–17%): Hyperkeratosis,
at reduced dose level (or permanently head­ache, pyrexia, arthralgia, alopecia,
discontinue). rash. Occasional (12%–10%): Back pain,
cough, myalgia, constipation, nasophar-
Dermatologic yngitis, fatigue.
Intolerable Grade 2 or any Grade
3 or 4 dermatologic toxicity: With- ADVERSE EFFECTS/TOXIC
hold treatment for up to 3 wks. If REACTIONS
improved, resume at reduced dose Cutaneous squamous cell carcinoma
level. If not improved, permanently (cuSCC) and keratoacanthomas reported
discontinue. in 7% of pts (esp. elderly, prior skin
cancer, chronic sun exposure). Skin
New Primary Malignancies reactions including palmar-plantar
Noncutaneous RAS mutation- erythrodysesthesia syndrome (PPES),
positive malignancies: Permanently papilloma have occurred. May increase
discontinue. cell proliferation of wild-type BRAF
Uveitis
melanoma or new malignant melano-
Uveitis (including iritis and iridocy-
mas. Eye conditions including uveitis,
clitis): If mild to moderate uveitis does
iritis reported. Hyperglycemia reported
not improve with ocular therapy or if in 6% of pts. Serious febrile drug reac-
severe uveitis occurs, withhold treatment tions including hypotension, rigors,
for up to 6 wks. If improved to Grade 1 dehydration reported in 4% of pts. Pts
or 0, resume at same dose (or at reduced with G6PD deficiency have increased risk
dose level). If not improved, permanently of hemolytic anemia. Pancreatitis, inter-
discontinue. stitial nephritis, bullous rash reported in
less than 10% of pts. Hemorrhagic events
Any Other Toxicity including GI bleeding, major organ
Intolerable Grade 2 or any Grade bleeding may occur in pts receiving con-
3 toxicity: Withhold treatment until comitant trametinib therapy. Cardiomy-
improved to Grade 1 or 0, then resume at opathy with an absolute decrease in LVEF
reduced dose level. If not improved, per- greater than 10% was reported.
manently discontinue. First occurrence
of any Grade 4 toxicity: Withhold
NURSING CONSIDERATIONS
treatment until improved to Grade 1 or BASELINE ASSESSMENT
0, then resume at reduced dose level (or Obtain BMP, blood glucose level; preg-
permanently discontinue). Recurrence nancy test in females if reproductive

underlined – top prescribed drug


dacomitinib 295
potential. Confirm presence of BRAF-
type mutation. Make note of current dacomitinib
moles, lesions for future comparison.
Conduct ophthalmologic exam, visual dak-oh-mi-ti-nib
acuity. Question current breastfeeding (Vizimpro)
status. Receive full medication his- Do not confuse dacomitinib D
tory (including herbal products) and with afatinib, dabrafenib, da-
screen for interactions. Offer emotional satinib, erlotinib, gefitinib, or
support. osimertinib.
INTERVENTION/EVALUATION uCLASSIFICATION
Monitor serum electrolytes; serum PHARMACOTHERAPEUTIC: Tyrosine
blood glucose periodically (esp. in pts kinase inhibitor. Epidermal growth
with diabetes). Obtain CBC if hemolytic factor receptor (EGFR) inhibitor.
anemia suspected in pts with G6PD CLINICAL: Antineoplastic.
deficiency. Monitor for signs of hyper-
glycemia. Assess skin for new moles,
lesions q2 mos during treatment and at USES
least 6 mos after discontinuation. Im- First-line treatment of metastatic non–
mediately report any vision changes, small-cell lung cancer (NSCLC) with
eye pain/swelling, febrile drug reac- EGFR exon 19 deletion or exon 21 L858R
tions, worsening renal function. Moni- substitution mutations.
tor I&Os. Consider echocardiogram in
PRECAUTIONS
pts suspected of cardiomyopathy, de-
creased LVEF. Contraindications: Hypersensitivity to
dacomitinib. Cautions: Baseline ane-
PATIENT/FAMILY TEACHING mia, leukopenia; dehydration, diabetes,
• Treatment may increase risk of new hepatic impairment; history of pulmo-
cancers. • Do not breastfeed. • Avoid nary disease.
pregnancy; nonhormonal contraception
should be used during treatment and up ACTION
to 2 wks after last dose. • Report Irreversibly inhibits kinase activity of
symptoms of high blood sugar levels human EGFR family and certain EGFR
(confusion, excessive thirst/hunger, mutations. Therapeutic Effect: Inhibits
headache, frequent urination); toxic tumor cell growth and metastasis.
skin reactions (itching, peeling, rash,
redness, swelling); eye pain/swelling, vi- PHARMACOKINETICS
sion changes; new moles or lesions of Widely distributed. Metabolized in liver.
the skin. • Fevers may be complicated Protein binding: 98%. Peak plasma
by low pressure, dehydration, or kidney concentration: 6 hrs. Excreted in feces
failure. • Minimize exposure to sun- (79%), urine (3%). Half-life: 70 hrs.
light. • Report bleeding of any
kind. • Therapy may reduce your LIFESPAN CONSIDERATIONS
heart’s ability to pump effectively; report Pregnancy/Lactation: Avoid preg-
difficulty breathing, chest pain, dizzi- nancy; may cause fetal harm. Female pts
ness, palpitations, swelling of the legs or of reproductive potential should use effec-
feet. • Do not take newly prescribed tive contraception during treatment and
medications unless approved by the for at least 17 days after discontinuation.
prescriber who originally started Unknown if distributed in breast milk.
treatment. Breastfeeding not recommended during
treatment and for at least 17 days after

Canadian trade name Non-Crushable Drug High Alert drug


296 dacomitinib
discontinuation. Children: Safety and Dermatologic Toxicity
efficacy not established. Elderly: May Grade 2 skin reaction: Withhold treat-
have higher risk of Grade 3 and 4 toxic ment until improved to Grade 1 or 0, then
reactions; higher frequency of treatment resume at same dose level. Recurrent
interruptions or discontinuation. or persistent Grade 2 skin reaction,
D Grade 3 or 4 skin reaction: Withhold
INTERACTIONS treatment until improved to Grade 1 or 0,
DRUG: Histamine H2 receptor antag- then resume at reduced dose level.
onists (e.g., famotidine), proton
pump inhibitors (e.g., omeprazole, GI Toxicity
pantoprazole) may decrease concen- Grade 2 diarrhea: Withhold treatment
tration/effect. May increase concentra- until improved to Grade 1 or 0, then
tion/effects of CYP2D6 substrates (e.g., resume at same dose level. Recurrent
amitriptyline, carvedilol, FLUox- Grade 2 diarrhea, Grade 3 or 4 diar-
etine, tamoxifen). HERBAL: None rhea: Withhold treatment until improved
significant. FOOD: None known. LAB to Grade 1 or 0, then resume at reduced
VALUES: May increase serum alkaline dose level.
phosphatase, ALT, AST, bilirubin, Pulmonary Toxicity
creatinine, glucose. May decrease Interstitial lung disease (ILD) of any
serum albumin, calcium, potassium, grade: Permanently discontinue.
sodium, magnesium; Hgb, Hct, lym-
phocytes, RBC count. Other Toxicities
Any other Grade 3 or 4 toxic
AVAILABILITY (Rx) reactions: Withhold treatment until
Tablets: 15 mg, 30 mg, 45 mg. improved to Grade 2 or less, then resume
at reduced dose level.
ADMINISTRATION/HANDLING
PO Dosage in Renal/Hepatic Impairment
• Give without regard to food. • If a Mild to moderate impairment: No
dose is missed or vomiting occurs after dose adjustment. Severe impairment:
administration, skip dose and give at Not specified; use caution.
next regularly scheduled time. • Give
at least 6 hrs before or at least 10 hrs SIDE EFFECTS
after H2 receptor antagonists (e.g., Frequent (87%–26%): Diarrhea, rash,
famotidine). paronychia, stomatitis, decreased appe-
tite, dry skin, xerosis, decreased weight.
INDICATIONS/ROUTES/DOSAGE Occasional (23%–7%): Alopecia, pru-
Non–Small-Cell Lung Cancer ritus, cough, nasal disorder (inflam-
PO: ADULTS, ELDERLY: 45 mg once daily. mation, epistaxis, mucosal disorder,
Continue until disease progression or rhinitis), conjunctivitis, nausea, extrem-
unacceptable toxicity. ity pain, constipation, dyspnea, asthenia,
musculoskeletal pain, mouth ulceration,
Reduction Schedule for Adverse insomnia, dermatitis, chest pain, fatigue,
Reactions vomiting, dysgeusia. Rare (2%–1%): Kera-
First dose reduction: 30 mg. Second titis, dehydration.
dose reduction: 15 mg.
ADVERSE EFFECTS/TOXIC
Dose Modification REACTIONS
Based on Common Terminology Criteria Anemia, lymphopenia is an expected
for Adverse Events (CTCAE). response to treatment. Nail reactions

underlined – top prescribed drug


dalbavancin 297
including nail infection, nail toxicity, terfere with absorption. Take dacomitinib
onychoclasis, onycholysis, onychoma- at least 6 hrs before or at least 10 hrs after
desis, paronychia reported in 64% of antacid. • Avoid prolonged sun expo-
pts. CTCAE Grade 3 or 4 skin reactions sure/tanning beds. Use high SPF sunscreen
occurred in 21% of pts. Upper respira- and lip balm to protect against sun-
tory tract infection reported in 12% of burn. • Report symptoms of liver prob- D
pts. Palmar-plantar erythrodysesthesia lems (abdominal pain, bruising, clay-
syndrome 15% of pts. Severe, sometimes colored stool, amber- or dark-colored
fatal, ILD/pneumonitis reported in 1% urine, yellowing of the skin or eyes); in-
of pts. flammation of the lung (excessive cough,
difficulty breathing, chest pain); toxic skin
NURSING CONSIDERATIONS reactions (itching, peeling, rash, redness,
BASELINE ASSESSMENT swelling), high blood sugar levels (e.g.,
blurry vision, confusion, frequent urina-
Obtain ANC, CBC, LFTs; pregnancy test tion, increased thirst, fruity breath).
in female pts of reproductive potential.
Question current breastfeeding status.
Confirm compliance of effective con-
traception. Question history of hepatic
impairment, pulmonary disease. Assess dalbavancin
skin for open wounds, lesions. Assess
hydration status. Receive full medication dal-ba-van-sin
history and screen for interactions. Offer (Dalvance)
emotional support. Do not confuse dalbavancin with
oritavancin or telavancin.
INTERVENTION/EVALUATION
uCLASSIFICATION
Monitor CBC, LFTs as clinically indicated.
Consider ABG, radiologic test if ILD/ PHARMACOTHERAPEUTIC: Glyco-
pneumonitis (excessive cough, dyspnea, peptide. CLINICAL: Antibiotic.
hypoxia) is suspected. Monitor daily
pattern of bowel activity, stool consis-
USES
tency. Antidiarrheal medication may be
needed to manage diarrhea. Assess skin Treatment of adult pts with acute bacte-
for dermal toxicities, rash; nail toxicities. rial skin and skin structure infections
Monitor for symptoms of hyperglycemia (ABSSSI) caused by susceptible strains of
(dehydration, confusion, excessive thirst, gram-positive microorganisms, including
Kussmaul respirations, polyuria). Moni- S. aureus (methicillin-susceptible and
tor I&Os, hydration status. methicillin-resistant strains), S. pyo-
genes, S. agalactiae, and S. anginosus
PATIENT/FAMILY TEACHING group (including S. anginosus, S. inter-
• Treatment may cause severe diarrhea, medius, S. constellatus).
which may require antidiarrheal medica-
tion. Report worsening of diarrhea or de- PRECAUTIONS
hydration. • Drink plenty of flu- Contraindications: Known hypersensi-
ids. • Avoid pregnancy. Female pts of tivity reaction to dalbavancin. Cautions:
childbearing potential should use reliable Hepatic/renal impairment, chronic hepa-
contraception during treatment and for at titis, hx alcohol abuse, hx hypersensitivity
least 17 days after last dose. Do not breast- reaction to glycopeptides (e.g., vanco-
feed during treatment and for at least 17 mycin), recent C. difficile infection or
days after last dose. • Antacids may in- antibiotic-associated colitis.

Canadian trade name Non-Crushable Drug High Alert drug


298 dalbavancin

ACTION bag may be refrigerated or stored at room


Inhibits cell wall synthesis by binding to temperature for up to 48 hrs. • Do not
bacterial cell membrane. Prevents cross- freeze.
linking and interferes with cell wall syn-
IV INCOMPATIBILITIES
thesis. Therapeutic Effect: Bactericidal.
D Do not infuse with other medications or
PHARMACOKINETICS electrolytes. Saline-based solutions may
Widely distributed. Metabolism not defined. cause precipitate formation. If using sin-
Protein binding: 93%. Primarily elimi- gle IV access, flush IV with 5% dextrose
nated in urine. Half-life: 14.4 days. before and after each use.

LIFESPAN CONSIDERATIONS INDICATIONS/ROUTES/DOSAGE


Pregnancy/Lactation: Unknown if dis­ Acute Bacterial Skin and Skin Structure
tributed in breast milk; use caution. Chil- Infection
dren: Safety and efficacy not established. IV: ADULTS/ELDERLY: (Two-Dose Regi-
Elderly: No age-related precautions noted. men): 1,000 mg once, followed by 500
mg once 7 days later. (Single-Dose
INTERACTIONS Regimen): 1,500 mg.
DRUG: None known. HERBAL: None
known. FOOD: None significant. LAB Dosage in Renal Impairment
VALUES: May increase serum ALT, AST, CrCl less than 30 mL/min in pts who
bilirubin. are not receiving regularly scheduled
hemodialysis: (Two-Dose Regimen):
AVAILABILITY (Rx) 750 mg once, followed by 375 mg once
Injection, Powder for Reconstitution: 7 days later. (Single-Dose Regimen):
500 mg. 1,125 mg. Pts receiving regularly
scheduled hemodialysis: No dose
ADMINISTRATION/HANDLING adjustment necessary.
IV
Dosage in Hepatic Impairment
b ALERT c Must be reconstituted with Mild impairment: No dose adjust­
Sterile Water for Injection and sub­ ment. Moderate to severe impairment:
sequently diluted with 5% Dextrose In- Not defined; use caution.
jection only.
Reconstitution • Reconstitute each SIDE EFFECTS
500-mg vial with 25 mL of Sterile Water Occasional (6%–4%): Nausea, vomiting,
for Injection for final concentration of 20 diarrhea, headache. Rare (3%–2%): Rash,
mg/mL. • To avoid foaming, alternate pruritus.
between gentle swirling and inversion of
vial until completely dissolved. Do not ADVERSE EFFECTS/TOXIC
shake. • Visually inspect for particulate REACTIONS
matter. Solution should appear clear, col- Serious hypersensitivity reactions in­clud­
orless to yellow. Do not use if particulate ing anaphylaxis or severe skin reactions
matter observed. • Aseptically transfer have been reported with glycopeptide
required dose into 5% dextrose to a final antibacterial agents. Too-rapid infu-
concentration of 1–5 mg/mL. sion may cause “red-man syndrome
Rate of administration • Infuse over reaction, characterized by flushing
30 min. of upper body, urticaria, pruritus, rash.
Storage • Store unused vials at room C. difficile–­ associated diarrhea with
temperature. • Reconstituted vials/diluted severity ranging from mild diarrhea to
fatal colitis has occurred. Drug-induced

underlined – top prescribed drug


dalfampridine 299
hepatotoxicity with hepatic enzymes
greater than 3 times upper limit of nor- dalfampridine
mal has been reported. Treatment in the
absence of proven or strongly suspected dal-fam-pri-deen
bacterial infection may increase risk of (Ampyra, Fampyra )
drug-resistant bacteria. Do not confuse Ampyra with D
anakinra, or dalfampridine with
NURSING CONSIDERATIONS desipramine.
BASELINE ASSESSMENT uCLASSIFICATION
Obtain baseline CBC, BMP, LFT, wound PHARMACOTHERAPEUTIC: Potassi-
culture and sensitivity, vital signs. Ques- um channel blocker. CLINICAL: Mul-
tion history of recent C. difficile infec- tiple sclerosis agent.
tion, hepatic/renal impairment, hyper­
sensitivity reaction. Assess skin wound
characteristics, hydration status. Ques- USES
tion pt’s usual stool characteristics Indicated to improve ambulation in pts
(color, frequency, consistency). with MS.
INTERVENTION/EVALUATION PRECAUTIONS
Assess skin infection/wound for im- Contraindications: Hypersensitivity to
provement. Monitor daily pattern of dalfampridine. History of seizures, mod-
bowel activity, stool consistency; in- erate to severe renal impairment (CrCl
creasing severity may indicate antibi- equal to or less than 50 mL/min). Cau-
otic-associated colitis. If frequent diar- tions: Mild renal impairment (CrCl equal
rhea occurs, obtain C. difficile toxin to 51–80 mL/min).
screen and initiate isolation precautions
until result confirmed. Encourage PO ACTION
intake. Monitor I&O. Monitor for “red- Improves conduction in demyelinated
man syndrome” during infusion; stop- axons by delaying repolarization and
ping or slowing infusion may decrease prolonging duration of action potentials.
reaction. Therapeutic Effect: Strengthens skel-
etal muscle fiber twitch activity; improves
PATIENT/FAMILY TEACHING
peripheral motor neurologic function.
• It is essential to complete drug therapy
despite symptom improvement. Early dis- PHARMACOKINETICS
continuation may result in antibacterial Rapidly absorbed from GI tract. Minimally
resistance or increased risk of recurrent metabolized in liver. Primarily excreted in
infection. • Report any episodes of diar- urine. Half-life: 5.2–6.5 hrs.
rhea, esp. following weeks after treatment
completion. Frequent diarrhea, fever, ab- LIFESPAN CONSIDERATIONS
dominal pain, blood-streaked stool may Pregnancy/Lactation: Unknown if drug
indicate infectious diarrhea, which may crosses placenta or is distributed in
be contagious to others. • Report ab- breast milk. Children: Safety and
dominal pain, black/tarry stools, bruis- efficacy not established. Elderly: Age-
ing, yellowing of skin or eyes, dark urine, related renal impairment may require
decreased urine output. • Do not dosage adjustment.
breastfeed. • Drink plenty of fluids.
INTERACTIONS
DRUG: None significant. HERBAL: None
significant. FOOD: None known. LAB VAL-
UES: May increase creatinine clearance.

Canadian trade name Non-Crushable Drug High Alert drug


300 dalteparin
PATIENT/FAMILY TEACHING
AVAILABILITY (Rx)
• Avoid tasks that require alertness, mo-
Tablet, Film-Coated, Extended-­Release: tor skills until response to drug is estab-
10 mg. lished. • Report difficulty in sleeping,
ADMINISTRATION/HANDLING dizziness, headache, nausea, back pain,
D loss of strength or energy. • Do not
PO chew, crush, dissolve, or divide tab-
• May give without regard to food. • Do lets. • Inform physician if ambulation
not break, crush, dissolve, or divide does not improve or worsens.
tablets.
INDICATIONS/ROUTES/DOSAGE
Multiple Sclerosis
PO: ADULTS 18 YRS AND OLDER, ELDERLY:
dalteparin
10 mg twice daily. Maximum: 20 mg/day. dal-te-par-in
Dosage in Renal Impairment (Fragmin)
CrCl 50 mL/min or less: Contra­ j BLACK BOX ALERT jEpidural
indicated. or spinal anesthesia greatly in-
creases potential for spinal or
Dosage in Hepatic Impairment epidural hematoma, subsequent
long-term or permanent paralysis.
No dose adjustment.
Do not confuse dalteparin with
SIDE EFFECTS heparin.
Frequent (9%–5%): Insomnia, dizziness, uCLASSIFICATION
headache, nausea, asthenia, back pain.
Rare (4%–2%): Paresthesia, nasopharyn- PHARMACOTHERAPEUTIC: Low mole­
gitis, constipation, dyspepsia, pharyngo- cular weight heparin. CLINICAL: An-
laryngeal pain. ticoagulant.

ADVERSE EFFECTS/TOXIC
REACTIONS USES
Urinary tract infection occurs in 12% Prevention of ischemic complications in
of pts. pts with unstable angina or non–Q-wave
MI. Prevention of deep vein thrombosis
NURSING CONSIDERATIONS (DVT) in pts undergoing hip replacement
surgery or in pts undergoing abdominal
BASELINE ASSESSMENT surgery who are at risk for thrombo-
Obtain CBC, BUN, creatinine clearance, embolic complications (e.g., pts older
serum chemistries prior to treatment and than 40 yrs, obese, pts with malignancy,
routinely thereafter. Conduct baseline history of DVT or PE, surgery requir-
neurologic exam. Assess motor func- ing general anesthesia and lasting more
tion, speech characteristics, gait, ability than 30 min). Extended treatment of
to ambulate. symptomatic venous thromboembolism
INTERVENTION/EVALUATION
(VTE) to reduce recurrence of VTE in
cancer pts. Prevention of DVT or pul-
Monitor CBC, serum chemistries, renal monary embolism in acutely ill pts with
function tests, particularly creatinine severely restricted mobility. Treatment of
clearance. Monitor for urinary, respira- symptomatic venous thromboembolism
tory infection. Assess for therapeutic re- (VTE) (e.g., DVT and/or PE) to reduce
sponse (improvement in walking as dem- the recurrence of VTE in infants 1 mo or
onstrated by increase in walking speed). older, children, and adolescents.

underlined – top prescribed drug


dalteparin 301

PRECAUTIONS FOOD: None known. LAB VALUES: May


Contraindications: Hypersensitivity to increase serum ALT, AST. May decrease
dalteparin, heparin, pork products; serum triglycerides.
active major bleeding; concurrent hepa-
AVAILABILITY (Rx)
rin therapy; unstable angina; history
of heparin-induced thrombocytopenia Injection, Solution:2,500 units/0.2 mL, D
(HIT), or HIT with thrombosis; non–Q- 5,000 units/0.2 mL, 7,500 units/0.3 mL,
wave MI; prolonged venous thromboem- 10,000 units/mL, 12,500 units/0.5 mL,
bolism undergoing epidural/neuraxial 15,000 units/0.6 mL, 18,000 units/0.72 mL.
anesthesia. Cautions: Conditions with
ADMINISTRATION/HANDLING
increased risk for hemorrhage, bacterial
endocarditis, renal/hepatic impairment, SQ
uncontrolled hypertension, history of • Visually inspect for particulate matter or
recent GI ulceration/hemorrhage, peptic discoloration. • Subcutaneously insert
ulcer disease, pericarditis, preexisting needle into abdomen, outer thigh, or upper
thrombocytopenia, recent childbirth, arm region and inject solution. • Do not
concurrent use of aspirin. inject into areas of active skin disease or
injury such as sunburns, rashes, inflamma-
ACTION tion, or infection. Rotate injection sites.
Antithrombin in presence of low molecu-
INDICATIONS/ROUTES/
lar weight heparin inhibits factor Xa,
DOSAGE
thrombin. Only slightly influences plate-
let aggregation, PT, aPTT. Therapeutic Non-Orthopedic Surgery
Effect: Produces anticoagulation. SQ: ADULTS, ELDERLY: 5,000 units 12
hrs before surgery (or evening before),
PHARMACOKINETICS then 5,000 units once daily. Continue
Route Onset Peak Duration until fully ambulatory and VTE risk has
SQ N/A 4 hrs N/A
diminished.

Protein binding: less than 10%. Half- Total Hip Surgery


life: 3–5 hrs. SQ: ADULTS, ELDERLY: 5,000 units once
daily (initial dose 12 or more hrs
LIFESPAN CONSIDERATIONS pre-operative or 12 or more hrs post-­
Pregnancy/Lactation: Use with caution, operative once hemostasis achieved) for
particularly during last trimester, immedi- 10–14 days up to 35 days.
ate postpartum period (increased risk of Unstable Angina, Non–Q-Wave MI
maternal hemorrhage). Unknown if distrib- SQ: ADULTS, ELDERLY: 120 units/kg q12h
uted in breast milk. Children: Safety and for up to 5–8 days (maximum: 10,000
efficacy not established. Elderly: No age- units/dose) given with aspirin. Discontinue
related precautions noted. dalteparin once clinically stable.
INTERACTIONS Venous Thromboembolism (Cancer Pts)
DRUG: NSAIDs (e.g., ibuprofen, SQ: ADULTS, ELDERLY: Initially (1 mo),
ketorolac, naproxen) may increase 200 units/kg (maximum: 18,000 units)
risk of bleeding. May increase effect of daily for 30 days. Maintenance (2–6
apixaban, dabigatran, edoxaban, mos): 150 units/kg once daily (maxi-
rivaroxaban. HERBAL: Herbals with mum: 18,000 units). If platelet count
anticoagulant/antiplatelet proper- 50,000–100,000 cells/mm3, reduce
ties (e.g., garlic, ginger, ginkgo dose by 2,500 units until platelet count
biloba) may increase risk of bleeding. recovers to 100,000 cells/mm3 or more.

Canadian trade name Non-Crushable Drug High Alert drug


302 dantrolene

If platelet count less than 50,000 cells/ rameters). Assess for any sign of bleeding
mm3, discontinue until platelet count (bleeding at surgical site, hematuria, blood
recovers to more than 50,000 cells/mm3. in stool, bleeding from gums, petechiae,
bruising/bleeding at injection sites). Moni-
Prevention of DVT, Acutely Ill Pt, Immobile tor for DVT (extremity pain, swelling, red-
D Pt ness), pulmonary embolism (chest pain,
SQ: ADULTS, ELDERLY: 5,000 units once dyspnea, hypoxia, tachycardia).
daily. Continue for length of hospital stay
PATIENT/FAMILY TEACHING
or until pt is fully ambulatory and VTE
risk has diminished. • Usual length of therapy is 5–10
days. • Do not take any OTC medica-
Treatment, Symptomatic VTE (Children) tion (esp. aspirin) without consulting
SQ: CHILDREN 8 YRS AND OLDER, ADOLES- physician. • Report bleeding, bruising,
CENTS: 100 units/kg/dose q12h. CHIL- dizziness, light-headedness, rash, itching,
DREN 2 YRS TO YOUNGER THAN 8 YRS: 125 fever, swelling, breathing difficulty. •
units/kg/dose q12h. INFANTS TO CHIL- Rotate injection sites daily. • Teach
DREN YOUNGER THAN 2 YRS: 150 units/kg/ proper injection technique. • Excessive
dose q12h. bruising at injection site may be lessened
by ice massage before injection. • Mon-
Dosage in Renal Impairment itor for symptoms of blood clots in the
For CrCl less than 30 mL/min, monitor anti- leg (extremity pain, swelling, redness) or
Xa levels to determine appropriate dose. blood clots in the lungs (chest pain, dif-
ficulty breathing, shortness of breath, fast
Dosage in Hepatic Impairment
heart rate).
No dose adjustment.
SIDE EFFECTS
Occasional (7%–3%): Hematoma
injection site. Rare (less than 1%): Hyper-
at
dantrolene
sensitivity reaction (chills, fever, pruritus,
dan-troe-leen
urticaria, asthma, rhinitis, lacrimation,
(Dantrium, Revonto, Ryanodex)
headache); mild, local skin irritation.
j BLACK BOX ALERT jPotential
ADVERSE EFFECTS/TOXIC for hepatotoxicity.
REACTIONS Do not confuse Dantrium
with danazol or Daraprim, or
Overdose may lead to bleeding complica- Revonto with Revatio.
tions ranging from local ecchymoses to
major hemorrhage. Thrombocytopenia uCLASSIFICATION
occurs rarely. PHARMACOTHERAPEUTIC: Calcium
NURSING CONSIDERATIONS release blocker. CLINICAL: Skeletal
muscle relaxant.
BASELINE ASSESSMENT
Obtain baseline coagulation studies, CBC,
esp. platelet count. Determine baseline USES
B/P. Screen for risk factors as listed in PO: Treatment of spasticity associated
Precautions. with upper motor neuron disorder (e.g.,
spinal cord injuries, CVA, cerebral palsy,
INTERVENTION/EVALUATION multiple sclerosis). Management of
Periodically monitor CBC, stool for occult malignant hyperthermia (MH), preven-
blood (no need for daily monitoring in pts tion of MH in susceptible individuals.
with normal presurgical coagulation pa- Parenteral: Management of malignant

underlined – top prescribed drug


dantrolene 303
hyperthermia. Prevention of malignant AVAILABILITY (Rx)
hyperthermia (preoperative/postopera- Capsules: 25 mg, 50 mg, 100 mg. Injec-
tive administration). OFF-LABEL: Neuro- tion, Powder for Reconstitution: 20-mg vial.
leptic malignant syndrome. Injection Suspension: 250 mg powder.

PRECAUTIONS ADMINISTRATION/HANDLING D
Contraindications: Hypersensitivity to dan­ IV
trolene. IV: None. PO: When spasticity
used to maintain posture/balance during Reconstitution • Reconstitute 20-mg
locomotion or to obtain increased motor vial with 60 mL Sterile Water for Injection
function. Active hepatic disease. Cau- (not Bacteriostatic Water for Injection).
tions: Cardiac/pulmonary impairment, his- (Ryanodex): 250-mg vial with 5 mL
tory of previous hepatic disease. Sterile Water for Injection.
Rate of administration • For thera-
ACTION peutic or emergency dose, give IV over
Interferes with release of calcium from 2–3 min. • For IV infusion, administer
sarcoplasmic reticulum of skeletal mus- over 1 hr. • Diligently monitor for extra­
cle. Prevents/reduces the increase in vasation (high pH of IV preparation). May
myoplasmic calcium ion concentration. produce severe complications. (Ryano-
Therapeutic Effect: Dissociates excita- dex): Do not dilute; infuse into IV catheter
tion-contraction coupling. Interferes with or indwelling catheter. Infuse over 1 min.
catabolic process associated with malig- Storage • Store at room tempera-
nant hyperthermia. ture. • Use within 6 hrs after reconsti-
tution. • Solution is clear, colorless.
PHARMACOKINETICS Discard if cloudy, precipitate forms.
Poorly absorbed from GI tract. Pro-
PO
tein binding: High. Metabolized in
• Give without regard to food.
liver. Primarily excreted in urine. Half-
life: IV: 4–8 hrs; PO: 8.7 hrs. IV INCOMPATIBILITIES
LIFESPAN CONSIDERATIONS D5W, 0.9% NaCl.
Pregnancy/Lactation: Readily crosses INDICATIONS/ROUTES/DOSAGE
placenta. Breastfeeding not recommended. Spasticity
Children: No age-related precautions
PO: ADULTS, ELDERLY: Initially, 25 mg once
noted in pts 5 yrs and older. Elderly: No daily for 7 days; then 25 mg 3 times/day for
precautions specified. 7 days; then 50 mg 3 times/day for 7 days;
then 100 mg 3 times/day. Maximum: 400
INTERACTIONS
mg/day. CHILDREN: Initially, 0.5 mg/kg/dose
DRUG: CNS depressants (e.g., LORaz- once daily for 7 days; then 0.5 mg/kg/dose
epam, morphine, zolpidem) may 3 times/day for 7 days; then 1 mg/kg/dose 3
increase CNS depression with short- times/day for 7 days; then 2 mg/kg/dose 3
term use. Strong CYP3A4 inducers times/day. Some pts may require dosing 4
(e.g., carBAMazepine, phenytoin, times/day. Maximum: 400 mg/day.
rifAMPin) may decrease concentration/
effect. HERBAL: Herbals with seda- Perioperative Prophylaxis for Malignant
tive properties (e.g., chamomile, Hyperthermic Crisis
kava kava, valerian) may increase CNS PO: ADULTS, ELDERLY, CHILDREN: 4–8 mg/
depression. St. John’s wort may decrease kg/day in 3–4 divided doses beginning
concentration/effect. FOOD: None known. 1–2 days before surgery; give last dose
LAB VALUES: May alter serum ALT, AST. 3–4 hrs before surgery.

Canadian trade name Non-Crushable Drug High Alert drug


304 DAPTOmycin
2.5 mg/
IV: ADULTS, ELDERLY, CHILDREN: PATIENT/FAMILY TEACHING
kg about 1.25 hrs before surgery with • Drowsiness usually diminishes with
additional doses as needed. continued therapy. • Avoid tasks that re-
quire alertness, motor skills until response
Management of Malignant Hyperthermic to drug is established. • Avoid alcohol/
D Crisis other depressants. • Report continued
IV: ADULTS, ELDERLY, CHILDREN: Initially, weakness, fatigue, nausea, diarrhea, skin
a minimum of 2.5 mg/kg rapid IV; may rash, itching, bloody/tarry stools.
repeat up to total cumulative dose of 10
mg/kg. May follow with 4–8 mg/kg/day
PO in 4 divided doses up to 3 days after
crisis. DAPTOmycin
Dosage in Renal/Hepatic Impairment dap-toe-mye-sin
No dose adjustment. Contraindicated (Cubicin)
with active hepatic disease. Do not confuse Cubicin with
Cleocin, or DAPTOmycin with
SIDE EFFECTS DACTINomycin.
Frequent: Drowsiness, dizziness, weak- uCLASSIFICATION
ness, general malaise, diarrhea (mild).
Occasional: Confusion, diarrhea (severe), PHARMACOTHERAPEUTIC: Cyclic lipo­
headache, insomnia, constipation, urinary peptide antibacterial agent. CLINI-
frequency. Rare: Paradoxical CNS excite- CAL: Antibiotic.
ment or restlessness, paresthesia, tinnitus,
slurred speech, tremor, blurred vision, USES
dry mouth, nocturia, impotence, rash,
pruritus. Treatment of complicated skin/skin
structure infections caused by suscep-
ADVERSE EFFECTS/TOXIC tible strains of gram-positive pathogens,
REACTIONS including S. aureus (methicillin suscep-
Risk of hepatotoxicity, most notably in tible and methicillin resistant [MRSA]),
females, pts 35 yrs and older, pts tak- S. pyogenes, S. agalactiae. Treatment of
ing other hepatotoxic medications con- S. aureus systemic infections caused by
currently. Overt hepatitis noted most methicillin-susceptible and methicillin-
frequently between 3rd and 12th mo of resistant S. aureus. OFF-LABEL: Severe
therapy. Overdose results in vomiting, infections caused by MRSA or vancomy-
muscular hypotonia, muscle twitching, cin-resistant Enterococcus (VRE); treat-
respiratory depression, seizures. ment of prosthetic joint infection caused
by staphylococci or Enterococcus.
NURSING CONSIDERATIONS PRECAUTIONS
BASELINE ASSESSMENT Contraindications: Hypersensitivity to
Obtain baseline LFT. Record onset, type, dapto­mycin. Cautions: Severe renal
location, duration of muscular spasm. impairment (CrCl less than 30 mL/min),
Check for immobility, stiffness, swelling. concurrent use of other medications
associated with myopathy (e.g., statins).
INTERVENTION/EVALUATION
Assist with ambulation. For pts on long- ACTION
term therapy, hepatic/renal function Binds to bacterial membranes and causes
tests, CBC should be performed periodi- rapid depolarization. Inhibits intracellu-
cally. Assess for therapeutic response: re- lar protein, DNA, RNA synthesis. Thera-
lief of pain, stiffness, spasm. peutic Effect: Bactericidal.
underlined – top prescribed drug
DAPTOmycin 305

PHARMACOKINETICS IV COMPATIBILITIES
Widely distributed. Protein binding: 90%. 0.9% NaCl, lactated Ringer’s, aztreo-
Primarily excreted unchanged in urine. nam (Azactam), DOPamine, fluconazole
Moderately removed by hemodialysis. (Diflucan), gentamicin, heparin, levo-
Half-life: 7–8 hrs (increased in renal FLOXacin (Levaquin).
impairment). D
INDICATIONS/ROUTES/DOSAGE
LIFESPAN CONSIDERATIONS Complicated Skin/Skin Structure
Pregnancy/Lactation: Unknown Infections
if drug is distributed in breast milk. IV: ADULTS, ELDERLY: 4 mg/kg every 24
Children: Safety and efficacy not hrs for 7–14 days.
established. Elderly: No age-related
precautions noted. Systemic Infections
IV: ADULTS, ELDERLY: 6–8 mg/kg once
INTERACTIONS daily for 2–6 wks.
DRUG: Concurrent use with HMG-CoA Dosage in Renal Impairment
reductase inhibitors (e.g., simvas- CrCl less than 30 mL/min, hemodi-
tatin) may cause myopathy. HERBAL: None alysis (HD), peritoneal dialysis (PD):
significant. FOOD: None known. LAB VAL- Dosage is 4 mg/kg q48h for skin and soft
UES: May increase CPK, serum potassium. tissue infections; 6 mg/kg q48h for staphy-
May alter LFT results. lococcal bacteremia. HD: Give dose after
dialysis. Continuous renal replacement
AVAILABILITY (Rx) therapy: Continuous venovenous
Injection, Powder for Reconstitution: 500 hemodialysis (CVVHD): 8 mg/kg q48h.
mg/vial. Continuous venovenous hemofiltra-
tion (CVVH) or continuous venove-
ADMINISTRATION/HANDLING nous hemodiafiltration (CVVHDF): 8
IV mg/kg q48h or 4–6 mg/kg q24h.
Reconstitution • Reconstitute 500- Dosage in Hepatic Impairment
mg vial with 10 mL 0.9% NaCl to provide No dose adjustment.
a concentration of 50 mg/mL. May fur-
ther dilute in 0.9% NaCl. • Do not SIDE EFFECTS
shake or agitate vial. Frequent (6%–5%): Constipation, nau-
Rate of administration • For IV sea, peripheral injection site reac-
injection, give over 2 min (concentration: tions, head­ache, diarrhea. Occasional
50 mg/mL). • For intermittent IV infu- (4%–3%): Insomnia, rash, vomiting.
sion (piggyback), infuse over 30 min. Rare (less than 3%): Pruritus, dizziness,
Storage • Refrigerate. • Appears as hypotension.
pale yellow to light brown lyophilized
cake. • Reconstituted solution is stable ADVERSE EFFECTS/TOXIC
for 12 hrs at room temperature or up to REACTIONS
48 hrs if refrigerated. • Discard if par- Skeletal muscle myopathy (muscle pain/
ticulate forms. weakness, particularly of distal extremi-
ties) occurs rarely. Antibiotic-associated
IV INCOMPATIBILITIES colitis (abdominal cramps, severe diar-
Diluents containing dextrose. If same IV rhea, fever), other superinfections may
line is used to administer different drugs, result from altered bacterial balance in
flush line with 0.9% NaCl. GI/GU tract.

Canadian trade name Non-Crushable Drug High Alert drug


306 daratumumab

NURSING CONSIDERATIONS inhibitor and an immunomodulatory


agent. In combination with dexametha-
BASELINE ASSESSMENT sone and either lenalidomide or bortezo-
Obtain CPK, blood cultures before first mib for treatment of multiple myeloma in
dose (therapy may begin before results are pts who have received at least one prior
D known). Question history of renal impair- therapy. In combination with pomalido-
ment. Screen for concomitant use of statins. mide and dexamethasone for treatment
of multiple myeloma in pts who have
INTERVENTION/EVALUATION received at least two prior therapies
Assess oral cavity for white patches on mu- including lenalidomide and a proteasome
cous membranes, tongue (thrush). Moni- inhibitor. Multiple myeloma (newly
tor for myopathy (muscle pain, weakness), diagnosed): Treatment of newly diag-
CPK levels, renal function tests. Monitor nosed multiple myeloma in combination
daily pattern of bowel activity, stool con- with bortezomib, melphalan, and predni-
sistency. Mild GI effects may be tolerable, SONE; newly diagnosed multiple myeloma
but increasing severity may indicate onset (in combination with lenalidomide and
of antibiotic-associated colitis. Be alert for dexamethasone) in pts ineligible for autol-
superinfection: fever, vomiting, diarrhea, ogous stem cell transplant.
anal/genital pruritus, oral mucosal changes
(ulceration, pain, erythema). Monitor for PRECAUTIONS
dizziness; institute appropriate measures. Contraindications: Hypersensitivity to
PATIENT/FAMILY TEACHING
daratumumab. Cautions: Obstructive
pulmo­nary disorders (e.g., COPD, emphy­
• Report rash, headache, nausea, dizzi- sema), baseline cytopenias, herpes zos-
ness, constipation, diarrhea, muscle ter infection, elderly.
pain, or any other new symptom.
ACTION
Binds to cell surface glycoprotein CD38
on CD38-expressing tumor cells (highly
daratumumab expressed on myeloma cells). Inhibits
tumor cell proliferation and induces
dar-a-toom-ue-mab apoptosis. Therapeutic Effect: Inhibits
(Darzalex) tumor cell growth and metastasis. Pro-
Do not confuse daratumumab motes tumor cell death.
with adalimumab, ofatumumab,
panitumumab, or necitumumab. PHARMACOKINETICS
uCLASSIFICATION
Widely distributed. Metabolism not
specified. Steady state reached approx.
PHARMACOTHERAPEUTIC: Anti-CD38 5 mos into the q4wk dosing period (by
monoclonal antibody. CLINICAL: An- 21st infusion). Elimination not specified.
tineoplastic. Half-life: 18 ± 9 days.
LIFESPAN CONSIDERATIONS
USES Pregnancy/Lactation: Avoid pregnancy;
Multiple myeloma (relapsed/refrac- may cause fetal harm/malformations.
tory): Monotherapy for the treatment Monoclonal antibodies are known to cross
of pts with multiple myeloma who have the placenta. Females of reproductive
received at least three prior lines of potential should use effective contracep-
therapy including a proteasome inhibitor tion during treatment and up to 3 mos
and an immunomodulatory agent or who after discontinuation. Unknown if dis-
are double-refractory to a proteasome tributed in breast milk. However, human

underlined – top prescribed drug


daratumumab 307
immunoglobulin G is present in breast milk. ticosteroid, acetaminophen, and an IV
Children: Safety and efficacy not estab- or oral antihistamine approx. 60 min
lished. Elderly: No age-related precau- before each infusion (see manufacturer
tions noted. guidelines). • Infuse using an in-line,
sterile, nonpyrogenic, low protein-bind-
INTERACTIONS ing polyethersulfone filter (0.22 or 0.2 D
DRUG: May decrease effect of BCG μm). • Infuse via dedicated line using
intravesical. HERBAL: None significant. infusion pump. • Do not administer as
FOOD: None known. LAB VALUES: Drug IV push or bolus. • Infusion should be
may be detected on both serum protein completed within 15 hrs. • If infusion
electrophoresis and immunofixation cannot be completed for any reason,
assays used to monitor multiple myeloma do not save unused portions for re-
endogenous M protein. May affect the use. • Postinfusion, administer an oral
determination of complete response corticosteroid on the first and second
and disease progression of some pts day after each infusion to reduce risk of
with immunoglobulin G kappa myeloma delayed infusion reactions (see manu-
protein. May cause positive Coombs’ test. facturer guidelines). • In pts with a
Expected to decrease Hgb, Hct, lympho- history of obstructive pulmonary disease,
cytes, neutrophils, platelets, RBCs. consider short-acting and long-acting
bronchodilators and an inhaled cortico-
AVAILABILITY (Rx) steroid postinfusion (may discontinue if
Injection Solution: 100 mg/5 mL, 400 no infusion reaction occurs after the first
mg/20 mL. four infusions).
Rate of administration • First infu­
ADMINISTRATION/HANDLING sion (1000 mL volume): Infuse at 50
IV mL/hr for the first 60 min. Increase in
increments of 50 mL/hr q1hr if no infu-
Preparation for administration • Cal- sion reactions occur. Maximum: 200
culate the dose and number of vials mL/hr. • Second infusion (500 mL
required based on weight in kg. • Solu- volume): Infuse at 50 mL/hr for the first
tion should appear colorless to pale 60 min. Increase in increments of 50 mL/
yellow. Do not use if opaque particles, hr q1hr if there were no Grade 1 or
discoloration, or foreign particles are greater infusion reactions during the
observed. • Remove a volume from the first 3 hrs of first infusion. Maximum:
0.9% NaCl infusion bag that is equal to 200 mL/hr. • Subsequent infusions
the required volume of the dose solution. (500 mL volume): Infuse at 100 mL/hr
• Dilute in 1000 mL (first infusion) or if there were no Grade 1 or greater infu-
500 mL (subsequent infusions) 0.9% sion reactions during a final infusion rate
NaCl bag. • Mix by gentle inversion. of greater than or equal to 100 mL/hr in
Do not shake or agitate. • Infusion the first two infusions. Increase in incre-
bags must be made of poly­vinylchloride, ments of 50 mL/hr q1hr if tolerated.
polypropylene, polyethylene, or poly- Maximum: 200 mL/hr.
olefin blend. • Diluted solution may Storage • Refrigerate unused vials.
develop very small translucent to white • Do not shake. • May refrigerate
proteinaceous particles; do not use diluted solution up to 24 hrs. • If
if diluted solution is discolored or if diluted solution is refrigerated, allow
visibly opaque or foreign particles are solution to warm to room temperature
observed. • Discard used portions of before use. • Protect from light.
vials.
Infusion guidelines • Prior to admin­ IV INCOMPATIBILITIES
istration, premedicate with an IV cor- Do not mix with other medications.
Canadian trade name Non-Crushable Drug High Alert drug
308 daratumumab

INDICATIONS/ROUTES/DOSAGE If Grade 3 reaction occurs for a third


Note: The initial dose (16 mg/kg on wk 1) time, permanently discontinue.
may be divided over 2 consecutive days Grade 4 reaction: Permanently dis­
(8 mg/kg/day on days 1 and 2 of wk 1 of continue.
therapy) to facilitate administration.
D Dosage in Renal Impairment
Multiple Myeloma (Relapsed/Refractory) No dose adjustment.
IV: ADULTS, ELDERLY: (Monotherapy
Dosage in Hepatic Impairment
or combination with lenalidomide/
Mild impairment: No dose adjustment.
dexamethasone or pomalidomide/
Moderate to severe impairment: Not
dexamethasone): Wks 1–8: 16 mg/
kg once wkly. Wks 9–24: 16 mg/kg specified; use caution.
once q2wks. Wk 25 and beyond: 16 SIDE EFFECTS
mg/kg once q4wks until disease progres-
sion. (Combination with bortezo- Frequent (37%–14%): Fatigue, back pain,
mib/dexamethasone): Wks 1–9: 16 nausea, pyrexia, cough, nasal congestion,
mg/kg once wkly. Wks 10–24: 16 mg/ arthralgia, diarrhea, dyspnea, decreased
kg q3wks for 5 doses. Wk 25 and appetite, extremity pain, constipation,
beyond: 16 mg/kg q4wks until disease vomiting. Occasional (12%–10%): Head-
progression. ache, musculoskeletal chest pain, chills,
hypertension.
Multiple Myeloma (Newly Diagnosed)
IV: ADULTS, ELDERLY: (In combination ADVERSE EFFECTS/TOXIC
with bortezomib, melphalan and REACTIONS
predniSONE): Wks 1–6: 16 mg/kg Anemia, leukopenia, neutropenia, throm-
once wkly. Wks 7–54: 16 mg/kg q3wks bocytopenia are expected responses to
for 16 doses. Wk 55 and beyond: 16 therapy. Infusion reactions occurred in
mg/kg q4wks until disease progression. approx. 50% of pts (mostly during first
(In combination with lenalidomide infusion). Infusion reactions can also occur
and low-dose dexamethasone): Wks with subsequent infusions (mainly during
1–8: 16 mg/kg once wkly for 8 doses. the infusion or within 4 hrs of completion).
Wks 9–24: 16 mg/kg once q2wks for 8 Severe infusion reactions may include
doses. Wks 25 and beyond: 16 mg/kg cough, dyspnea, bronchospasm, hyperten-
once q4wks until disease progression. sion, hypoxia, laryngeal edema, pulmonary
edema, wheezing. Less common reactions
Dose Modification may include chills, headache, hypotension,
Infusion Reactions rash, nausea, pruritus, urticaria, vomiting.
Promptly interrupt infusion if any reac- Infections including pneumonia, upper
tion occurs. respiratory tract infection, nasopharyngitis
Grade 1 or 2 reaction: Once symptoms reported in 20%–11% of pts. Herpes zoster
resolve, resume infusion at a decreased reported in 3% of pts. Thrombocytopenia
rate that is 50% (or less) of previous rate. may increase risk of bleeding.
If no further reactions are observed, may
increase infusion rate as appropriate. NURSING CONSIDERATIONS
Grade 3 reaction: If symptoms resolve BASELINE ASSESSMENT
to Grade 2 or less, consider resuming
Obtain CBC, blood type and screen; vital
infusion at a decreased rate that is 50%
signs. Obtain pregnancy test in female pts
(or less) of previous rate. If no further
of reproductive potential. Question his-
reactions are observed, may increase
tory of COPD, emphysema, herpes infec-
rate as appropriate. If a Grade 3 reaction
tion; prior hypersensitivity reaction to any
recurs, decrease rate as outlined earlier.
drug in treatment regimen; prior infusion
underlined – top prescribed drug
darbepoetin alfa 309
reaction. Assess nutritional status. Screen Do not confuse Aranesp with
for active infection. Offer emotional sup- Aricept, or darbepoetin with
port. dalteparin or epoetin.
INTERVENTION/EVALUATION uCLASSIFICATION
Monitor CBC, vital signs periodically. Ad- PHARMACOTHERAPEUTIC: Eryth- D
minister in an environment equipped to ropoiesis stimulating agent (ESA).
monitor for and manage infusion reactions. CLINICAL: Hematopoietic agent.
If infusion reaction of any grade/severity
occurs, immediately interrupt infusion and
manage symptoms. Accurately record char- USES
acteristics of infusion reactions (severity, Treatment of anemia associated with
type, time of onset). Reactions may affect chronic renal failure (including pts on
future infusion rates. To prevent herpes dialysis and pts not on dialysis), treat-
zoster reactivation in pts with prior history, ment of anemia caused by concurrent
consider antiviral prophylaxis within 1 wk myelosuppressive chemotherapy in
of starting treatment and continue for 3 pts planned to receive chemotherapy
mos following discontinuation. Monitor for for minimum of 2 additional months.
infection. Monitor daily pattern of bowel ac- OFF-LABEL: Treatment of symptomatic
tivity, stool consistency. anemia in myelodysplastic syndrome
PATIENT/FAMILY TEACHING
(MDS).
• Blood levels will be monitored periodi- PRECAUTIONS
cally. • Treatment may depress your im- Contraindications: Hypersensitivity to dar­
mune system and reduce your ability to fight bepoetin. Pure red cell aplasia that begins
infection. Report symptoms of infection such after treatment with darbepoetin alfa or
as body aches, chills, cough, fatigue, fever. other erythropoietin protein medication.
Avoid those with active infection. • Avoid Uncontrolled hypertension. Cautions: His-
pregnancy. Do not breastfeed. • Effective tory of seizures, hypertension. Not rec-
contraception is recommended during treat- ommended in pts with mild to moderate
ment and for at least 3 mos after final anemia and HF or CAD.
dose. • Severe infusion reactions can oc-
cur at any time. Immediately report symp- ACTION
toms of infusion reactions such as chills, Stimulates division and differentiation
cough, difficulty breathing, headache, hives, of committed erythroid progenitor
itching, nausea, rash, stuffy or runny nose, cells; increases release of reticulo-
throat tightness, vomiting, wheezing. cytes from bone marrow into blood-
stream. Therapeutic Effect: Induces
erythropoiesis.
darbepoetin alfa
PHARMACOKINETICS
dar-be-poe-e-tin al-fa Well absorbed after SQ administration.
(Aranesp) Half-life: 48.5 hrs.
j BLACK BOX ALERT j
Increased risk of serious cardio- LIFESPAN CONSIDERATIONS
vascular events, thromboembolic Pregnancy/Lactation: Unknown if drug
events, mortality, time-to-tumor
progression when administered to a crosses placenta or is distributed in
target hemoglobin greater than 11 g/ breast milk. Children: Safety and
dL. Shortened overall survival and/ efficacy not established. Elderly: Age-
or increased risk of tumor progres- related renal impairment may require
sion has been reported with breast, dosage adjustment.
cervical, head/neck, NSCL cancers.
Canadian trade name Non-Crushable Drug High Alert drug
310 darbepoetin alfa

INTERACTIONS Decrease dose by 25%: If Hgb


DRUG: Contraceptives (e.g., estradiol, approaches 12 g/dL or increases greater
levonorgestrel), estrogens may in­crease than 1 g/dL in any 2-wk period.
risk of thrombosis. HERBAL: None sig- Increase dose by 25%: If Hgb does
nificant. FOOD: None known. LAB VAL- not increase by 1 g/dL after 4 wks of
D UES: May decrease serum ferritin, serum therapy and Hgb is below target range
transferrin saturation. (with adequate iron stores). Do not
increase dose more frequently than
AVAILABILITY (Rx) every 4 wks.
25 mcg/mL, 40 mcg/
Injection Solution: Note: If pt does not attain Hgb range
mL, 60 mcg/mL, 100 mcg/mL, 200 mcg/ of 10–12 g/dL after appropriate dos-
mL, 300 mcg/mL. Prefilled Syringe: 10 ing over 12 wks, do not increase dose
mcg/0.4 mL, 25 mcg/0.42 mL, 40 mcg/0.4 and use minimum effective dose to
mL, 60 mcg/0.3 mL, 100 mcg/0.5 mL, maintain Hgb level that will avoid red
150 mcg/0.3 mL, 200 mcg/0.4 mL, 300 blood cell transfusions. Discontinue
mcg/0.6 mL, 500 mcg/mL. treatment if responsiveness does not
improve.
ADMINISTRATION/HANDLING
Anemia Associated with Chemotherapy
IV b ALERT c Initiate only if Hgb less
Preparation • Avoid excessive agita- than 10 g/dL and anticipated duration
tion of vial; do not shake (will cause of myelosuppression is 2 months or
foaming). Do not dilute. longer. Titrate dose to maintain Hgb
Rate of administration • May be level and avoid RBC transfusions. Dis-
given as IV bolus. continue upon completion of chemo-
Storage • Refrigerate. • Do not therapy.
shake. Vigorous shaking may denature SQ: ADULTS, ELDERLY: 2.25 mcg/kg once
medication, rendering it inactive. wkly or 500 mcg every 3 wks.
Increase dose: If Hgb does not increase
SQ by 1 g/dL after 6 wks and remains below
• Use 1 dose per vial; do not reenter 10 g/dL, increase dose to 4.5 mcg/kg
vial. Discard unused portion. once wkly. No dose adjustment if using
q3wk dosing.
IV INCOMPATIBILITIES Decrease dose: Decrease dose by 40%
Do not mix with other medications. if Hgb increases greater than 1 g/dL in
any 2-wk period or Hgb reaches level that
INDICATIONS/ROUTES/DOSAGE will avoid red blood cell transfusions.
Anemia in Chronic Renal Failure Note: Withhold dose when Hgb exceeds
b ALERT c Individualize dosing and use a level needed to avoid RBC transfusions;
lowest dose to reduce need for RBC trans- resume at dose 40% lower when Hgb
fusions. On Dialysis: Initiate when Hgb approaches a level where transfusions
less than 10 g/dL; reduce or stop dose may be required.
when Hgb approaches or exceeds 11 g/dL.
Not on Dialysis: Initiate when Hgb less Dosage in Renal/Hepatic Impairment
than 10 g/dL and Hgb decline would likely No dose adjustment.
result in RBC transfusion; reduce dose or
stop if Hgb exceeds 10 g/dL. SIDE EFFECTS
IV, SQ: ADULTS, ELDERLY: On Dialysis: Frequent: Myalgia, hypertension/hypo-
Initially, 0.45 mcg/kg once wkly or 0.75 tension, headache, diarrhea. Occasional:
mcg/kg once q2wks. Not on Dialy- Fatigue, edema, vomiting, reaction at
sis: 0.45 mcg/kg q4wks. injection site, asthenia, dizziness.

underlined – top prescribed drug


darifenacin 311

ADVERSE EFFECTS/TOXIC USES


REACTIONS Management of symptoms of bladder
Cardiovascular events, including CVA, overactivity (urge incontinence, urinary
MI, venous thromboembolism, vascular urgency/frequency).
access device thrombosis, mortality, may
occur when given to target hemoglobin PRECAUTIONS D
greater than 11 g/dL or during rapid rise Contraindications: Hypersensitivity to dari-
in hemoglobin. Hypersensitivity reac- fenacin. Pts with or at risk of uncontrolled
tions, including anaphylaxis, may occur. narrow-angle glaucoma, gastric reten-
Cases of anemia and pure red cell aplasia tion, urine retention. Cautions: Bladder
may occur in pts with chronic renal dis- outflow obstruction, hepatic impairment,
ease when given subcutaneously. nonobstructive prostatic hyperplasia,
decreased GI motility (e.g., severe consti-
NURSING CONSIDERATIONS pation, ulcerative colitis), GI obstructive
BASELINE ASSESSMENT disorders, controlled narrow-angle glau-
coma, myasthenia gravis, concurrent use
Establish baseline CBC (esp. note Hgb, of strong CYP3A4 inhibitors. Hot weather
Hct). Assess B/P before drug administra- and/or exercise.
tion. B/P often rises during early therapy in
pts with history of hypertension. Assess se- ACTION
rum iron (transferrin saturation should be Acts as a direct antagonist at muscarinic
greater than 20%), serum ferritin (greater receptor sites in cholinergically inner-
than 100 ng/mL) before and during ther- vated organs; limits bladder contractions.
apy. Consider supplemental iron therapy. Therapeutic Effect: Reduces symp-
INTERVENTION/EVALUATION toms of bladder irritability/overactivity
Monitor CBC, Hgb, reticulocyte count, serum (urge incontinence, urinary urgency/
BUN, creatinine, ferritin, potassium, phos- frequency), improves bladder capacity.
phate. Monitor B/P aggressively for increase PHARMACOKINETICS
(25% of pts taking medication require an-
tihypertension therapy, dietary restrictions). Well absorbed following PO administra-
tion. Protein binding: 98%. Metabolized
PATIENT/FAMILY TEACHING in liver. Excreted in urine (60%), feces
• Frequent blood tests needed to deter- (40%). Half-life: 13–19 hrs.
mine correct dose. • Report swollen
extremities, breathing difficulty, extreme LIFESPAN CONSIDERATIONS
fatigue, or severe headache. • Avoid Pregnancy/Lactation: Unknown if drug
tasks requiring alertness, motor skills crosses placenta or is distributed in
until response to drug is established. breast milk. Children: Safety and effi-
cacy not established. Elderly: No age-
related precautions noted.
darifenacin INTERACTIONS
dare-i-fen-a-sin DRUG: Strong CYP3A4 inhibitors (e.g.,
(Enablex) clarithromycin, ketoconazole, ritona-
vir) may increase concentration/effects.
uCLASSIFICATION Strong CYP3A4 inducers (e.g., car-
PHARMACOTHERAPEUTIC: Mus- BAMazepine, phenytoin, rifAMPin)
carinic receptor antagonist. Anticho- may decrease concentration/effect.
linergic agent. CLINICAL: Urinary Anticholinergics (e.g., aclidinium,
anti­spasmodic. ipratropium, tiotropium, umecli-
dinium) may increase anticholinergic
Canadian trade name Non-Crushable Drug High Alert drug
312 darunavir
effect. May increase concentration/ INTERVENTION/EVALUATION
effect of thioridazine. HERBAL: None Monitor I&O. Palpate bladder and use
significant. FOOD: None known. LAB VAL- bladder scanner to assess for urine re-
UES: None known. tention. Monitor daily pattern of bowel
activity, stool consistency for evidence of
D AVAILABILITY (Rx) constipation. Dry mouth may be relieved
Tablets (Extended-Release): 7.5 mg, with sips of water. Assess for relief of
15 mg. symptoms of overactive bladder (urge in-
continence, urinary frequency/urgency).
ADMINISTRATION/HANDLING
PATIENT/FAMILY TEACHING
PO
• Give without regard to food. • • Swallow tablet whole; do not chew,
Administer extended-release tablets crush, dissolve, or divide. • Increase
whole; do not break, crush, dissolve, or fluid intake to reduce risk of constipa-
divide tablet. tion. • Avoid tasks that require alert-
ness, motor skills until response to drug
INDICATIONS/ROUTES/DOSAGE is established.
Overactive Bladder
PO: ADULTS, ELDERLY: Initially, 7.5 mg
once daily. If response is not adequate
after at least 2 wks, may increase to 15 darunavir
mg once daily. Do not exceed 7.5 mg
once daily in moderate hepatic impair- dar-ue-na-veer
ment or concurrent use with strong or (Prezista)
potent CYP3A4 inhibitors (e.g., clarithro- FIXED-COMBINATION(S)
mycin, fluconazole, protease inhibitors).
Prezcobix: Darunavir/cobicistat (an-
Dosage in Renal Impairment tiretroviral booster): 800 mg/150 mg.
No dose adjustment.
uCLASSIFICATION
Dosage Hepatic Impairment
PHARMACOTHERAPEUTIC: Protease
Moderate impairment: Maximum:
7.5 mg. Severe impairment: Not reco­ inhibitor (anti-HIV). CLINICAL: Anti­
mmended. retroviral.

SIDE EFFECTS
USES
Frequent (35%–21%): Dry mouth, consti-
pation. Occasional (8%–4%): Dyspepsia, Treatment of HIV infection in combina-
headache, nausea, abdominal pain. Rare tion with ritonavir and other antiretro-
(3%–2%): Asthenia, diarrhea, dizziness,
viral agents in adults and children 3 yrs
ocular dryness. and older.

ADVERSE EFFECTS/TOXIC PRECAUTIONS


REACTIONS Contraindications: Hypersensitivity to
UTI occurs occasionally. darunavir. Concurrent therapy with
alfuzosin, colchicine (in pts with renal
NURSING CONSIDERATIONS and/or hepatic impairment), dihydro-
ergotamine, dronedarone, elbasvir/
BASELINE ASSESSMENT grazoprevir, ergonovine, ergotamine,
Monitor voiding pattern, assess signs/ lovastatin, lurasidone, methylergono-
symptoms of overactive bladder prior to vine, oral midazolam, pimozide, ranola-
therapy as baseline. zine, rifAMPin, sildenafil (for treatment

underlined – top prescribed drug


darunavir 313
of PAH), simvastatin, St. John’s wort, cholesterol, triglycerides, uric acid. May
triazolam. Cautions: Diabetes, hemo- decrease lymphocytes/neutrophil count,
philia, known sulfonamide allergy, platelets, WBC count; serum bicarbon-
hepatic impairment. ate, albumin, calcium. May alter serum
glucose, sodium.
ACTION D
Binds to site of HIV-I protease activity, AVAILABILITY (Rx)
inhibiting cleavage of viral precursors into Suspension, Oral: (Prezista): 100 mg/mL
functional proteins required for infec- Tablets: (Prezista): 75 mg, 150 mg,
tious HIV. Therapeutic Effect: Prevents 600 mg, 800 mg.
formation of mature viral cells.
ADMINISTRATION/HANDLING
PHARMACOKINETICS PO
Readily absorbed following PO admin- • Give with food (increases plasma con-
istration. Metabolized in liver. Protein centration). • Coadministration with
binding: 95%. Excreted in feces (80%), ritonavir required. • Do not break,
urine (14%). Not significantly removed crush, dissolve, or divide film-coated tab-
by hemodialysis. Half-life: 15 hrs. lets. • Shake suspension prior to each
dose. Use provided oral dosing syringe.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if drug INDICATIONS/ROUTES/DOSAGE
crosses placenta or is distributed in Note: Genotypic testing recommended
breast milk. Breastfeeding not recom- in therapy-experienced pts.
mended. Children: Safety and efficacy
not established in pts younger than 3 HIV Infection, Treatment Experienced
yrs. Elderly: No age-related precautions PO: ADULTS, ELDERLY: (With 1 or more
noted. darunavir resistance–associated sub­
stitution): 600 mg administered twice
INTERACTIONS daily with 100 mg ritonavir twice daily.
DRUG: May increase concentration/effect (With no darunavir resistance–­
of amiodarone, axitinib, bosutinib, associated substitutions): 800 mg with
budesonide, cochicine, droneda- 100 mg ritonavir or 150 mg cobicistat
rone, eletriptan, ergot derivatives once daily.
(e.g., ergotamine), fluticasone
(nasal), lovastatin, midazolam, HIV Infection, Treatment Naive
nimodipine, ranolazine, rego- PO: ADULTS, ELDERLY: 800 mg adminis-
rafenib, simvastatin, thioridazine. tered with 100 mg ritonavir or 150 mg
Strong CYP3A4 inducers (e.g., car- cobicistat once daily.
BAMazepine, phenytoin, rifAMPin)
may decrease concentration/effect. Usual Dosage During Pregnancy
Strong CYP3A4 inhibitors (e.g., car- PO: ADULTS: 600 mg administered twice
BAMazepine, ketoconazole, ritona- daily with 100 mg ritonavir twice daily.
vir) may increase concentration/effect.
May decrease effects of methadone, Usual Pediatric Dose
oral contraceptives. HERBAL: Gar- Treatment naive or treatment experi-
lic, St. John’s wort may lead to loss of enced with no darunavir resistance–
virologic response, potential resistance associated substitutions: (Once-daily
to darunavir. FOOD: Food increases Dosing) (Suspension Only): WEIGH-
plasma concentration. LAB VALUES: May ING 14 KG: 490 mg with 96 mg ritonavir.
increase aPTT, PT, serum alkaline phos- 13 KG: 455 mg with 80 mg ritonavir. 12
phatase, bilirubin, amylase, lipase, KG: 420 mg with 80 mg ritonavir. 11 KG:

Canadian trade name Non-Crushable Drug High Alert drug


314 darunavir
385 mg with 64 mg ritonavir. 10 KG: inhibitors. Drug-induced hepatotoxicity
350 mg with 64 mg ritonavir. was reported, esp. in pts with advanced
(Suspension or Tablets): WEIGHING HIV disease, cirrhosis, hepatitis B or
40 KG OR MORE: 800 mg with 100 mg C virus infection, or pts taking mul-
ritonavir. 30–39 KG: 675 mg with 100 mg tiple medications. May increase risk of
D ritonavir. 15–29 KG: 600 mg with 100 mg bleeding in pts with history of hemo-
ritonavir. philia A or B. Immune reconstitution
syndrome (inflammatory response to
Treatment Experienced with 1 or More dormant opportunistic infections such
Darunavir Resistance–Associated as Mycobacterium avium, cytomega-
Substitution lovirus, PCP, tuberculosis, or accelera-
Use Tablet or Suspension tion of autoimmune disorders such as
PO: CHILDREN WEIGHING 40 KG OR MORE: Graves’ disease, polymyositis, Guillain-
600 mg twice daily with 100 mg ritonavir. Barré) may occur. Skin reactions
WEIGHING 30–39 KG: 450 mg twice daily with (including Stevens-Johnson syndrome,
60 mg ritonavir. WEIGHING 15–29 KG: 375 toxic epidermal necrolysis) occur
mg twice daily with 48 mg ritonavir. rarely. Hypersensitivity reactions includ-
ing anaphylaxis, angioedema, broncho-
Use Oral Suspension Only spasm may occur.
WEIGHING 14 KG TO LESS THAN 15 KG: 280
mg (48 mg ritonavir) twice daily. 13 KG TO NURSING CONSIDERATIONS
LESS THAN 14 KG: 260 mg (40 mg rito-
BASELINE ASSESSMENT
navir) twice daily. 12 KG TO LESS THAN 13
KG: 240 mg (40 mg ritonavir) twice daily. Obtain CD4+ count, viral load, HIV RNA
11 KG TO LESS THAN 12 KG: 220 mg (32 mg level. Confirm HIV genotype. Question
ritonavir) twice daily. 10 KG TO LESS THAN 11 history of diabetes, hemophilia, hepatic
KG: 200 mg (32 mg ritonavir) twice daily. impairment, prior hypersensitivity reac-
tions. Receive full medication history
Dosage in Renal Impairment (including herbal products); screen for
Mild to severe impairment: No dose contraindications/interactions. Offer emo­
adjustment. tional support.
Dosage in Hepatic Impairment INTERVENTION/EVALUATION
Mild to moderate impairment: No Monitor CD4+ count, viral load, HIV
dose adjustment. Severe impairment: RNA level for treatment effectiveness.
Not recommended. Monitor BMP, LFT, renal function, se-
rum blood glucose periodically. An in-
SIDE EFFECTS crease in serum creatinine greater than
Frequent (19%–13%): Diarrhea, nausea, 0.4 mg/dL from baseline may indicate
headache, nasopharyngitis. Occasional renal impairment. Closely monitor for
(3%–2%): Constipation, abdominal pain, GI discomfort. Monitor daily pattern of
vomiting. Rare (less than 2%): Allergic der- bowel activity, stool consistency. Moni-
matitis, dyspepsia, flatulence, abdominal tor for hepatotoxicity (bruising, hema-
distention, anorexia, arthralgia, myalgia, turia, jaundice, right upper abdominal
paresthesia, memory impairment. pain, nausea, vomiting, weight loss),
hypersensitivity reactions. Assess skin
ADVERSE EFFECTS/TOXIC for rash, other skin reactions. Assess
REACTIONS for immune reconstitution syndrome,
Hyperglycemia, exacerbation of diabe- opportunistic infections (onset of fever,
tes, diabetic ketoacidosis, new-onset oral mucosa changes, cough, other re-
diabetes have been reported in protease spiratory symptoms).

underlined – top prescribed drug


dasatinib 315
PATIENT/FAMILY TEACHING CML with resistance, intolerance to prior
• There is a high risk of drug interactions therapy, including imatinib. Treatment of
with other medications. Do not take newly Philadelphia chromosome–positive (Ph+)
prescribed medications unless approved by CML in chronic phase of newly diagnosed
prescriber who originally started treatment. pt. (Children): Treatment of Ph+ CML
Do not take herbal products, esp. St. John’s in chronic phase. Acute lymphoblastic D
wort. • If amiodarone therapy cannot be leukemia: Treatment of adults with Ph+
withheld or stopped, immediately report acute lymphoblastic leukemia (ALL) with
symptoms of slow heart rate such as chest resistance or intolerance to prior therapy,
pain, confusion, dizziness, fainting, light- including imatinib. (Children): Treat-
headedness, memory problems, palpita- ment of newly diagnosed Ph+ ALL. OFF-
tions, weakness. • Therapy is not a cure LABEL: Post–stem cell transplant follow-up
for HIV infection, nor does it reduce risk of treatment of CML. Treatment of GI stromal
transmission. • Report any skin reac- tumor.
tions. • Report any signs of decreased
urine output, abdominal pain, yellowing of PRECAUTIONS
skin or eyes, darkened urine, clay-colored Contraindications: Hypersensitivity to
stools, weight loss. • As immune system da­satinib. Cautions: Hepatic impair-
strengthens, it may respond to dormant in- ment, myelosuppression (particu-
fections hidden within the body. Report any larly thrombocytopenia), pts prone to
new fever, chills, body aches, cough, night fluid retention, those with prolonged
sweats, shortness of breath. Antiretrovirals QT interval, cardiovascular/pulmonary
may cause excess body fat in the upper disease. Concomitant use of anticoagu-
back, neck, breast, and trunk and may lants, CYP3A4 inducers/inhibitors may
cause decreased body fat in legs, arms, and increase risk of pulmonary arterial
face. • Drug resistance can form if ther- hypertension.
apy is interrupted for even a short time; do
not run out of supply. • Report symptoms ACTION
of high blood sugar levels (confusion, ex- Reduces activity of proteins responsible
cessive thirst/hunger, headache, frequent for uncontrolled growth of leukemia cells
urination). by binding to most imatinib-resistant
BCR-ABL mutations of pts with CML or
ALL. Therapeutic Effect: Inhibits pro-
dasatinib liferation, tumor growth of CML and ALL
cancer cell lines.
da-sa-ti-nib
(Sprycel) PHARMACOKINETICS
Do not confuse dasatinib with Extensively distributed in extravascular
erlotinib, imatinib, or lapatinib. space. Protein binding: 96%. Metabo-
lized in liver. Eliminated primarily in
uCLASSIFICATION feces. Half-life: 3–5 hrs.
PHARMACOTHERAPEUTIC: BCR-ABL
tyrosine kinase inhibitor. CLINICAL: LIFESPAN CONSIDERATIONS
Antineoplastic. Pregnancy/Lactation: Has potential
for severe teratogenic effects, fertility
impairment. Breastfeeding not recom-
USES mended. Children: Safety and efficacy
Chronic myeloid leukemia (CML): not established in pts younger than 18
(Adults): Treatment of chronic, acceler- yrs. Elderly: No age-related precau-
ated, myeloid or lymphoid blast phase of tions noted.

Canadian trade name Non-Crushable Drug High Alert drug


316 dasatinib

INTERACTIONS phase: 140 mg once daily. May increase


DRUG: CYP3A4 inhibitors (e.g., to 180 mg once daily in pts not achieving
clarithromycin, ketoconazole, rito- cytogenetic response.
navir) may increase concentration/
Ph+CML (Newly Diagnosed in Chronic
effect. CYP3A4 inducers (e.g., car-
D BAMazepine, phenytoin, rifAMPin)
Phase)
PO: ADULTS, ELDERLY: 100 mg once
may decrease concentration/effect. May
daily. May increase to 140 mg/day in pts
decrease therapeutic effect of BCG (intra-
not achieving cytogenetic response. CHIL-
vesical), vaccines (live). H2 antago-
DREN (1 YR AND OLDER) WEIGHING 45 KG OR
nists (e.g., famotidine), proton
MORE: 100 mg once daily. May increase
pump inhibitors (e.g., omeprazole,
to 120 mg once daily. 30–44 KG: 70 mg
pantoprazole) may decrease concentra-
once daily. May increase to 90 mg once
tion/effect. May increase adverse effects
daily. 20–29 KG: 60 mg once daily. May
of vaccines (live). HERBAL: Echina-
increase to 70 mg once daily. 10–19
cea may decrease therapeutic effect. St.
KG: 40 mg once daily. May increase to 50
John’s wort may decrease concentration/
mg once daily.
effect. FOOD: Grapefruit products may
increase concentration/toxicity (increa­sed Ph+ ALL
risk of torsades, myelotoxicity). LAB VAL- PO: ADULTS, ELDERLY: 140 mg once
UES: May decrease WBC, platelets, Hgb, daily. May increase to 180 mg once daily
Hct, RBC; serum calcium, phosphates. in pts not achieving cytogenetic response.
May increase serum ALT, AST, bilirubin, CHILDREN WEIGHING 10 KG OR MORE, ADO-
creatinine. LESCENTS WEIGHING 45 KG OR MORE: 100
mg once daily. 30 TO LESS THAN 45 KG: 70
AVAILABILITY (Rx) mg once daily. 20 TO LESS THAN 30 KG: 60
Tablets (Film-Coated): 20 mg, 50 mg once daily. 10 TO LESS THAN 20 KG: 40
mg, 70 mg, 80 mg, 100 mg, 140 mg. mg once daily.
ADMINISTRATION/HANDLING Dosage in Renal/Hepatic Impairment
PO No dose adjustment.
• Give without regard to food. • Take SIDE EFFECTS
with food or large glass of water if GI
Frequent (50%–32%): Fluid retention,
upset occurs. • Avoid grapefruit prod-
ucts. • Do not break, crush, dissolve, or diarrhea, headache, fatigue, musculo-
divide film-coated tablets. • Do not give skeletal pain, fever, rash, nausea, dys-
antacids either 2 hrs prior to or within 2 pnea. Occasional (28%–12%): Cough,
hrs after dasatinib administration. abdominal pain, vomiting, anorexia,
asthenia, arthralgia, stomatitis, dizziness,
INDICATIONS/ROUTES/DOSAGE constipation, peripheral neuropathy,
Note: CYP3A4 inhibitors: Consider myalgia. Rare (less than 12%): Abdomi-
decreasing dose from 100 mg to 20 mg nal distention, chills, weight increase,
or 140 mg to 40 mg. CYP3A4 induc- pruritus.
ers: Consider increasing dose with ADVERSE EFFECTS/TOXIC
monitoring. REACTIONS
CML (Resistant or Intolerant) Pleural effusion occurred in 8% of pts,
PO: ADULTS, ELDERLY: Chronic phase: febrile neutropenia in 7%, GI bleeding,
100 mg once daily. May increase to 140 pneumonia in 6%, thrombocytopenia in
mg once daily in pts not achieving cyto- 5%, dyspnea in 4%; anemia, cardiac fail-
genetic response. Accelerated or blast ure in 3%.

underlined – top prescribed drug


DAUNOrubicin 317

NURSING CONSIDERATIONS uCLASSIFICATION

BASELINE ASSESSMENT PHARMACOTHERAPEUTIC: Anthra-


cycline topoisomerase II inhibitor.
Obtain CBC weekly for first mo, bi- CLINICAL: Antineoplastic.
weekly for second mo, and periodi-
cally thereafter. Monitor LFT before D
treatment begins and monthly thereaf- USES
ter. Obtain baseline weight. Offer emo- Cerubidine: Treatment of leukemias
tional support. (acute lymphocytic [ALL], acute myeloid
INTERVENTION/EVALUATION [AML]) in combination with other agents.
Assess lower extremities for pedal edema, PRECAUTIONS
early evidence of fluid retention. Weigh
Contraindications: Hypersensitivity to
daily, monitor for unexpected rapid
weight gain. Offer antiemetics to control DAUNO­­rubicin. Cautions: Preexisting heart
nausea, vomiting. Monitor daily pattern disease or bone marrow suppression, hy-
of bowel activity, stool consistency. Assess pertension, concurrent chemotherapeutic
oral mucous membranes for evidence of agents, elderly, infants, radiation therapy.
stomatitis. Monitor CBC for neutropenia, ACTION
thrombocytopenia; monitor hepatic func-
tion tests for hepatotoxicity. Inhibits DNA and RNA synthesis by inter-
calation between DNA base pairs and by
PATIENT/FAMILY TEACHING steric obstruction. Cell cycle–phase non-
• Avoid crowds, those with known infec- specific. Therapeutic Effect: Prevents
tion. • Avoid contact with anyone who cell division.
recently received live virus vaccine; do
not receive vaccinations. • Antacids PHARMACOKINETICS
may be taken up to 2 hrs before or 2 hrs Widely distributed. Protein binding: High.
after taking dasatinib. • Avoid grape- Does not cross blood-brain barrier.
fruit products. • Do not chew, crush, Metabolized in liver. Excreted in urine
dissolve, or divide tablets. (40%); biliary excretion (40%). Half-
life: 18.5 hrs; metabolite: 26.7 hrs.
LIFESPAN CONSIDERATIONS
DAUNOrubicin Pregnancy/Lactation: If possible, avoid
use during pregnancy, esp. first trimester.
daw-noe-roo-bi-sin May cause fetal harm. Breastfeeding not
(Cerubidine) recommended. Children: Cardiotoxicity
j BLACK BOX ALERT j May may be more frequent and occur at lower
cause cumulative, dose-related my- cumulative doses. Elderly: Cardiotoxic-
ocardial toxicity. Severe myelosup- ity may be more frequent; reduced bone
pression may lead to infection or marrow reserves require caution. Age-
hemorrhage. Must be administered related renal impairment may require
by personnel trained in administra-
tion/handling of chemotherapeutic dosage adjustment.
agents. Caution in pts with renal
impairment or hepatic dysfunction. INTERACTIONS
Extravasation may cause severe DRUG: Bevacizumab, cyclophos-
local tissue necrosis. phamide may increase risk of cardio-
Do not confuse DAUNOrubicin toxicity. Bone marrow depressants
with DACTINomycin, DOXOru- (e.g., cladribine) may enhance
bicin, epiRUBicin, IDArubicin, myelosuppression. Live virus vac-
or valrubicin. cines may potentiate virus replication,
Canadian trade name Non-Crushable Drug High Alert drug
318 DAUNOrubicin
increase vaccine side effects, decrease 550 mg/m2 in adults (increased risk of
pt’s antibody response to vaccine. cardiotoxicity) or 400 mg/m2 in those
HERBAL: Echinacea may de­ crease receiving chest irradiation.
level/effects. FOOD: None known. LAB
VALUES: May increase serum alkaline Acute Lymphocytic Leukemia
D phosphatase, bilirubin, uric acid, AST. IV: ADULTS, ELDERLY: 45 mg/m2on days
1, 2, and 3 (in combination with vin-
AVAILABILITY (Rx) CRIStine, predniSONE, asparaginase).
Injection Solution: (Cerubidine): 5 mg/mL. CHILDREN 2 YRS AND OLDER AND BODY
Injection Solution: (DaunoXome): 2 mg/mL. SURFACE AREA 0.5 m2 OR GREATER: 25 mg/
m2 on day 1 of every wk for up to 4–6
ADMINISTRATION/HANDLING cycles (in combination with vinCRIStine,
IV (Cerubidine)
predniSONE). CHILDREN YOUNGER THAN
2 YRS, OR BODY SURFACE AREA LESS THAN
Give by IV push or IV infusion. 0.5 m2: 1 mg/kg/dose on day 1 of every
Reconstitution • May further dilute wk for up to 4 to 6 cycles (in combina-
with 100 mL D5W or 0.9% NaCl. tion with vinCRIStine, predniSONE).
Rate of administration • For IV
push, withdraw desired dose into syringe Acute Myeloid Leukemia
containing 10–15 mL 0.9% NaCl. Inject IV: ADULTS YOUNGER THAN 60 YRS: 45
over 1–5 min into tubing of rapidly mg/m2 on days 1, 2, and 3 of induction
infusing IV solution of D5W or 0.9% course, then on days 1 and 2 of subsequent
NaCl. • For IV infusion, further dilute courses (in combination with cytarabine).
with 100 mL D5W or 0.9% NaCl. Infuse ADULTS 60 YRS AND OLDER: 30 mg/m2 on
over 15–30 min. • Extravasation days 1, 2, and 3 of induction course, then
produces immediate pain, severe local on days 1 and 2 of subsequent courses (in
tissue damage. Aspirate as much infiltrated combination with cytarabine).
drug as possible, then infiltrate area with
Dosage in Renal Impairment
hydrocortisone sodium succinate injection
Serum creatinine greater than 3
(50–100 mg hydrocortisone) and/or
mg/dL: 50% of normal dose.
isotonic sodium thiosulfate injection
or ascorbic acid injection (1 mL of 5% Dosage in Hepatic Impairment
injection). Apply cold compresses. Bilirubin 1.2–3 mg/dL: 75% of normal
Storage • Refrigerate intact vi­ als. dose. Bilirubin 3.1–5 mg/dL: 50% of
• Protect from light. • Solutions pre- normal dose. Bilirubin greater than 5
pared for infusion stable for 24 hrs at mg/dL: DAUNOrubicin is not recom-
room temperature. mended for use in this pt population.
IV INCOMPATIBILITIES SIDE EFFECTS
Allopurinol (Aloprim), aztreonam (Azac- Frequent: Complete alopecia (scalp, axil-
tam), cefepime (Maxipime), dexametha- lary, pubic), nausea, vomiting (beginning
sone (Decadron), heparin, piperacillin a few hrs after administration and last-
and tazobactam (Zosyn). ing 24–48 hrs). Occasional: Diarrhea,
IV COMPATIBILITIES abdominal pain, esophagitis, stomatitis,
transverse pigmentation of fingernails,
Granisetron (Kytril), ondansetron (Zo­­ toenails. Rare: Transient fever, chills.
fran).
ADVERSE EFFECTS/TOXIC
INDICATIONS/ROUTES/DOSAGE REACTIONS
b ALERT c Refer to individual proto- Myelosuppression manifested as hema-
cols. Cumulative dose should not exceed tologic toxicity (severe leukopenia,
underlined – top prescribed drug
deferasirox 319
anemia, thrombocytopenia) is expected. hygiene. • Do not have immunizations
Decreases in platelet count, WBC count without physician’s approval (drug low-
occur in 10–14 days, then return to ers resistance). • Avoid contact with
normal level by third week. Cardiotoxic- those who have recently received live vi-
ity including absolute decrease in LVEF, rus vaccine. • Promptly report fever,
HF, death may occur, esp. in children sore throat, signs of local infection, un- D
and pts with preexisting cardiac disease. usual bruising/bleeding from any site,
ECG findings and/or cardiomyopathy is yellowing of whites of eyes/skin, difficulty
manifested as HF (risk increases when breathing. • Report persistent nausea,
cumulative dose exceeds 550 mg/m2 in vomiting. • Treatment may impair the
adults, 300 mg/m2 in children 2 yrs and heart’s ability to pump blood effectively;
older, or total dosage greater than 10 report difficulty breathing, chest pain,
mg/kg in children younger than 2 yrs). palpitations, swelling of the legs or feet.
Pericarditis-myocarditis may occur. Sec-
ondary leukemias were reported in pts
exposed to topoisomerase II inhibitors
when used concomitantly with other
antineoplastics or radiation therapy. deferasirox
Extravasation can cause severe local tis-
sue necrosis. dee-fur-a-sir-ox
(Exjade, Jadenu)
NURSING CONSIDERATIONS j BLACK BOX ALERT jMay
cause renal/hepatic failure,
BASELINE ASSESSMENT hepatotoxicity, gastrointestinal
Obtain CBC, LFT; BUN, serum creati- hemorrhage.
nine, CrCl, GFR in pts with renal impair- Do not confuse deferasirox with
ment. Obtain ECG before initiation, esp. deferoxamine.
in pts with cardiac disease. Antiemetics uCLASSIFICATION
may be effective in preventing, treating
nausea. Ensure patency of IV access. PHARMACOTHERAPEUTIC: Iron-
Obtain accurate height and weight chelating agent. CLINICAL: Iron re-
for dose calculation. Offer emotional duction agent.
support.
INTERVENTION/EVALUATION USES
Obtain CBC frequently; BMP, LFT, serum Treatment of chronic iron overload due to
uric acid periodically. Monitor daily pat- blood transfusions (transfusional hemo-
tern of bowel activity, stool consistency. siderosis) in pts 2 yrs and older or due to
Monitor for hematologic toxicity (fever, non–transfusion-dependent thalassemia
sore throat, signs of local infection, un- syndrome in pts 10 yrs and older.
usual bruising/bleeding from any site);
symptoms of anemia (excessive fatigue, PRECAUTIONS
weakness). Diligently monitor for ex- Contraindications: Hypersensitivity to
travasation, tissue necrosis. deferasirox. Platelet counts less than
50,000 cells/mm3; poor performance sta-
PATIENT/FAMILY TEACHING tus, high-risk myelodysplastic syndromes
• Urine may turn reddish color for 1–2 or advanced malignancies; CrCl less than
days after beginning therapy. • Hair 40 mL/min or serum creatinine greater
loss is reversible, but new hair growth than 2 times the upper limit of normal.
may have different color, texture. New Cautions: Renal/hepatic impairment,
hair growth resumes about 5 wks after elderly, concurrent medications that may
last therapy dose • Maintain strict oral increase GI effects (e.g., NSAIDs).
Canadian trade name Non-Crushable Drug High Alert drug
320 deferasirox

ACTION INDICATIONS/ROUTES/DOSAGE
Selective for iron. Binds iron with high Iron Overload Due to Transfusions
affinity in a 2:1 ratio. Therapeutic PO: ADULTS, ELDERLY, CHILDREN 2 YRS AND
Effect: Induces iron excretion through OLDER: (Exjade): Initially, 20 mg/kg once
the feces. daily. Maintenance: (Titrate to individual
D response and goals.) Adjust dosage by 5
PHARMACOKINETICS or 10 mg/kg/day every 3–6 mos based on
Well absorbed following PO administra- serum ferritin levels. Consider holding for
tion. Protein binding: 99%. Metabolized serum ferritin less than 500 mcg/L. Maxi-
in liver. Excreted in feces (84%), urine mum: 40 mg/kg once daily. (Jadenu):
(8%). Half-life: 8–16 hrs. Initially, 14 mg/kg once daily. Mainte-
nance: (Titrate to individual response and
LIFESPAN CONSIDERATIONS goals.) Adjust dosage by 3.5 or 7 mg/kg/
Pregnancy/Lactation: Unknown if drug day based on serum ferritin levels. Consider
crosses placenta or is distributed in breast holding for serum ferritin less than 500
milk. Children: Not recommended for mcg/L. Maximum: 28 mcg/kg once daily.
pts younger than 2 yrs. Elderly: No age-
related precautions noted. Thalassemia Syndromes
PO: ADULTS, ELDERLY, CHILDREN 10 YRS
INTERACTIONS AND OLDER: (Exjade): Initially, 10 mg/kg
DRUG: Antacids containing alumi­ once daily. May increase to 20 mg/kg once
nium may decrease concentration/effects. daily after 4 wks if baseline iron is greater
May increase concentration/effect of the- than 15 mg Fe/g dry wgt. (Jadenu): Ini-
ophylline, tiZANidine. HERBAL: None tially, 7 mg/kg once daily. May increase
significant. FOOD: Bioavailability is variably to 14 mg/kg/day after 4 wks if baseline
increased when given with food. LAB VAL- iron greater than 15 mg Fe/g dry wgt.
UES: Decreases serum ferritin. May increase Maintenance: (Exjade/Jadenu): Dose
serum ALT, AST, creatinine; urine protein. adjustments based on serum ferritin and
hepatic iron concentrations.
AVAILABILITY (Rx)
Dosage in Renal Impairment
Packets, Sprinkle: (Jadenu): 90 mg,
180 mg, 360 mg. Tablets: (Jadenu): 90 Note: See Contraindications.
ADULTS: For increase in serum creati-
mg, 180 mg, 360 mg. Tablets, Soluble:
(Exjade): 125 mg, 250 mg, 500 mg.
nine greater than 33% on 2 consecutive
measures, reduce daily dose by 10 mg/kg.
ADMINISTRATION/HANDLING CHILDREN: For increase in serum creati-

PO
nine above age-appropriate upper limit of
• Give on empty stomach 30 min before normal on 2 consecutive measures, reduce
food. • Do not give simultaneously with daily dose by 10 mg/kg. CrCl 40–60 mL/
aluminum-containing antacids, chole- min: Reduce starting dose by 50%.
styramine. • Tablets for suspension Dosage in Hepatic Impairment
should not be chewed or swallowed For severe or persistent elevations in
whole. • Disperse tablet by stirring in hepatic function tests, consider dose
water, apple juice, orange juice until fine reduction or discontinuation. Moderate
suspension is achieved. • Dosage less impairment: Reduce initial dose by 50%.
than 1 g should be dispersed in 3.5 oz of
liquid, dosage more than 1 g should be SIDE EFFECTS
dispersed in 7 oz of liquid. If any residue Frequent (19%–10%): Fever, headache,
remains in glass, resuspend with a small abdominal pain, cough, nasopharyngitis,
amount of liquid. • Give regular tablets diarrhea, nausea, vomiting. Occasional
whole with water.
underlined – top prescribed drug
denosumab 321
(9%–4%): Rash, arthralgia, fatigue, back USES
pain, urticaria. Rare (1%): Edema, sleep Prolia: Treatment of osteoporosis in
disorder, dizziness, anxiety. postmenopausal women at high risk for
ADVERSE EFFECTS/TOXIC fracture. Treatment of glucocorticoid-
REACTIONS induced osteoporosis in pts at high risk of
fracture who are receiving an equivalent D
Bronchitis, pharyngitis, acute tonsillitis, dose of 7.5 mg or more of predniSONE
ear infection occur occasionally. Hepati- for duration of at least 6 mos. Treatment
tis, auditory disturbances, ocular abnor- to increase bone mass in men at high
malities occur rarely. Acute renal failure, risk for fractures; treatment of bone loss
cytopenias (e.g., agranulocytosis, neutro- in men receiving androgen deprivation
penia, thrombocytopenia) may occur. therapy for nonmetastatic prostate cancer
NURSING CONSIDERATIONS and in women at high risk for fractures
receiving adjuvant aromatase inhibitor
BASELINE ASSESSMENT therapy for breast cancer. Xgeva: Pre-
Obtain baseline serum CBC, ferritin, iron, vention of skeletal-related events (e.g.,
creatinine, ALT, AST, urine protein, then fracture, spinal cord compression) in pts
monthly thereafter. Auditory, ophthalmic with bone metastases from solid tumor
testing should be obtained before therapy or multiple myeloma. Treatment of giant
and annually thereafter. cell tumor of bone in adults and skel-
etally mature adolescents. Treatment of
INTERVENTION/EVALUATION hypercalcemia of malignancy refractory
Treatment should be interrupted if serum to bisphosphonate therapy. OFF-LABEL:
ferritin levels are consistently less than Treatment of bone destruction caused by
500 mcg/L. Suspend treatment if severe rheumatoid arthritis.
rash occurs.
PRECAUTIONS
PATIENT/FAMILY TEACHING
Contraindications: Hypersensitivity to
• Take on empty stomach 30 min before deno­sumab. Prolia: Preexisting hypo-
food. • Do not chew or swallow soluble calcemia, pregnancy. Xgeva: Preexisting
tablets; disperse tablet completely in water, hypocalcemia. Cautions: History of hypo-
apple juice, orange juice; drink resulting parathyroidism, thyroid/parathyroid sur-
suspension immediately. • Do not take gery, malabsorption syndromes, excision
aluminum-containing antacids concur- of small intestine, immunocompromised
rently. • Report severe skin rash, changes pts. Pts with severe renal impairment or
in vision/hearing, or yellowing of skin/eyes. receiving dialysis (greater risk for devel-
oping hypocalcemia). Pts with impaired
immune system or immunosuppressive
denosumab therapy.

den-oh-sue-mab ACTION
(Prolia, Xgeva) Binds to RANKL; blocks interaction
Do not confuse denosumab between RANKL and RANK, prevent-
with daclizumab, or Prolia with ing osteoclast formation. Therapeutic
Avandia or Zebeta. Effect: Decreases bone resorption;
increases bone mass in osteoporosis;
uCLASSIFICATION decreases skeletal-related events and
PHARMACOTHERAPEUTIC: Monoclo- tumor-induced bone destruction in solid
nal antibody (with affinity for RANKL). tumors, multiple myeloma. Inhibits
CLINICAL: Bone-modifying agent. tumor growth.

Canadian trade name Non-Crushable Drug High Alert drug


322 denosumab

PHARMACOKINETICS Dosage in Renal/Hepatic Impairment


Serum level detected 1 hr after adminis- No dose adjustment.
tration. Half-life: 32 days. SIDE EFFECTS
LIFESPAN CONSIDERATIONS Frequent (35%–12%): Back pain, extrem-
D ity pain. Occasional (8%–5%): Musculo-
Pregnancy/Lactation: Approved for
skeletal pain, vertigo, peripheral edema,
use only in postmenopausal women.
sciatica. Rare (4%–2%): Bone pain,
Children: Approved for use only in
upper abdominal pain, rash, insomnia,
postmenopausal women. Elderly: No
flatulence, pruritus, myalgia, asthenia,
age-related precautions noted.
GI reflux.
INTERACTIONS ADVERSE EFFECTS/TOXIC
DRUG: May enhance adverse/toxic effect REACTIONS
of belimumab, immunosuppressants. Increases risk of infection, specifically
HERBAL: None significant. FOOD: None cystitis, upper respiratory tract infection,
known. LAB VALUES: May decrease serum pneumonia, pharyngitis, herpes zoster
calcium. May increase serum cholesterol. (shingles) occur in 2%–6% of pts. Osteo-
AVAILABILITY (Rx) necrosis of the jaw (OJN) was reported.
Suppression of bone turnover, pancreati-
Injection, Solution: (Prolia): 60 mg/mL. tis have been reported.
(Xgeva): 120 mg/1.7 mL.
NURSING CONSIDERATIONS
ADMINISTRATION/HANDLING
SQ BASELINE ASSESSMENT
• Administer in upper arm, upper thigh, Hypocalcemia must be corrected prior
or abdomen. to treatment. Calcium 1,000 mg/day
Storage • Refrigerate. Use within 14 and vitamin D at least 400 international
days once at room temperature. • Solu- units/day should be given. Dental exam
tion appears as clear, colorless to pale should be provided prior to treat-
yellow. ment. Recommend baseline bone density
scan.
INDICATIONS/ROUTES/DOSAGE
INTERVENTION/EVALUATION
Note: Administer calcium and vitamin D
to prevent/treat hypocalcemia. Monitor serum magnesium, calcium,
ionized calcium, phosphate. In pts pre-
Prolia disposed with hypocalcemia and distur-
Androgen Deprivation, Bone Loss, bances of mineral metabolism, clinical
Osteoporosis monitoring of calcium, mineral levels
SQ: ADULTS, ELDERLY: 60 mg every 6 mos. is highly recommended. Adequately
supplement all pts with calcium and
Xgeva vitamin D. Monitor for delayed fracture
Prevention of Skeletal-Related Events healing.
from Solid Tumors, Multiple Myeloma
PATIENT/FAMILY TEACHING
SQ: ADULTS, ELDERLY: 120 mg q4wks.
• Report rash, new-onset eczema. • Seek
Giant Cell Tumor of Bone, Hypercalcemia prompt medical attention if signs, symp-
of Malignancy toms of severe infection (rash, itching,
SQ: ADULTS, ELDERLY, MATURE ADOLES- reddened skin, cellulitis) occur. • Report
CENTS: 120 mg q4wks with additional muscle stiffness, numbness, cramps,
doses on days 8 and 15 of first mo of spasms (signs of hypocalcemia); swelling
therapy. or drainage from jaw, mouth, or teeth.

underlined – top prescribed drug


desmopressin 323
decreasing urine volume. Increases
desmopressin levels of von Willebrand factor, fac-
tor VIII, tissue plasminogen activator
des-moe-press-in (tPA). Therapeutic Effect: Shortens
(DDAVP, DDAVP Rhinal Tube, activated partial thromboplastin time
­Noctiva, Stimate) (aPTT), bleeding time. Decreases uri- D
nary output.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Synthetic PHARMACOKINETICS
vasopressin analog (hormone, pos-
Route Onset Peak Duration
terior pituitary). CLINICAL: Anti-
hemophilic. Hemostatic. PO 1 hr 2–7 hrs 8–12 hrs
IV 15–30 min 1.5–3 hrs 8–12 hrs
Intrana- 15 min–1 1–5 hrs 8–12 hrs
sal hr
USES
Nasal, Parenteral: Antidiuretic Poorly absorbed after PO, nasal admin-
replacement therapy in managing cen- istration. Metabolism: Unknown. Half-
tral cranial diabetes insipidus. Manage life: PO: 1.5–2.5 hrs. Intranasal:
polyuria and polydipsia following head 3.3–3.5 hrs. IV: 0.4–4 hrs.
trauma or surgery in pituitary region.
Maintain hemostasis and control bleed- LIFESPAN CONSIDERATIONS
ing in hemophilia A, von Willebrand’s Pregnancy/Lactation: Unknown if dis-
disease (type I). PO: Antidiuretic tributed in breast milk. Children: Cau-
replacement therapy in managing cen- tion in neonates, pts younger than 3 mos
tral cranial diabetes insipidus, primary (increased risk of fluid balance prob-
management of nocturnal enuresis, lems). Careful fluid restrictions recom-
management of temporary polyuria, mended in infants. Elderly: Increased
polydipsia following pituitary surgery risk of hyponatremia, water intoxication.
or head trauma. OFF-LABEL: Uremic
bleeding occurring with acute/chronic INTERACTIONS
renal failure; prevent surgical bleeding DRUG: CarBAMazepine, lamoTRIgine,
in pts with uremia. NSAIDs (e.g., ibuprofen, ketorolac,
naproxen), SSRIs (e.g., citalopram,
PRECAUTIONS sertraline), tricyclic antidepressants
Contraindications: Hypersensitivity to (e.g., amitriptyline, doxepin, nor-
des­mo­pressin. Hyponatremia, history of triptyline) may increase effect. Deme-
hyponatremia, moderate to severe renal clocycline, lithium may decrease effect.
impairment. Cautions: Predisposition Corticosteroids (e.g., dexametha-
to thrombus formation; conditions with sone, predniSONE), loop diuret-
fluid, electrolyte imbalance; coronary ics (e.g., furosemide) may increase
artery disease; hypertensive cardiovascu- hyponatremic effect. HERBAL: None sig-
lar disease, elderly pts, cystic fibrosis, HF, nificant. FOOD: None known. LAB VAL-
renal impairment, polydipsia. Avoid use UES: May decrease serum sodium.
in hemophilia A with factor VIII levels
less than 5%; hemophilia B; severe type AVAILABILITY (Rx)
I, type IIB, platelet-type von Willebrand’s
Injection Solution: (DDAVP): 4 mcg/mL.
disease.
Nasal Solution: (DDAVP Rhinal Tube 0.01%):
ACTION 100 mcg/mL (10 mcg/spray). Nasal Spray:
(Stimate): 1.5 mg/mL (150 mcg/spray).
Increases cAMP in renal tubular cells,
Tablets: (DDAVP): 0.1 mg, 0.2 mg.
which increases water permeability,

Canadian trade name Non-Crushable Drug High Alert drug


324 desmopressin

ADMINISTRATION/HANDLING YRS: Initially, 5 mcg (0.05 mL)/day.


Range: 5–30 mcg (0.05–0.3 mL)/day as
IV a single or 2 divided doses.
Reconstitution • For IV infusion,
Hemophilia A, Von Willebrand’s Disease
dilute in 10–50 mL 0.9% NaCl (10 mL for
D children 10 kg or less; 50 mL for adults,
(Type I)
IV infusion: ADULTS, ELDERLY, CHIL-
children greater than 10 kg).
DREN: 0.3 mcg/kg as slow infusion.
Rate of administration • Infuse over
Intranasal: (Use 1.5 mg/mL Concen-
15–30 min.
tration Providing 150 mcg/Spray):
Storage • Refrigerate.
ADULTS, ELDERLY, CHILDREN WEIGHING
SQ MORE THAN 50 KG: 300 mcg; use 1 spray
• Withdraw dose from vial. Further dilu- in each nostril. ADULTS, ELDERLY, CHIL-
tion not required. DREN WEIGHING 50 KG OR LESS: 150 mcg
as a single spray. Repeat use based on
Intranasal clinical conditions/laboratory work.
• Refrigerate DDAVP Rhinal Tube solu-
tion, Stimate nasal spray. • Rhinal Tube Dosage in Renal Impairment
solution, Stimate nasal spray are stable CrCl less than 50 mL/min: Not
for 3 wks at room tempera- recommended.
ture. • DDAVP nasal spray is stable at
Dosage in Hepatic Impairment
room temperature. • Calibrated cathe-
ter (rhinyle) is used to draw up mea- No dose adjustment.
sured quantity of desmopressin; with one SIDE EFFECTS
end inserted in nose, pt blows on other
end to deposit solution deep in nasal cav- Occasional: IV: Pain, redness, swelling
ity. • For infants, young children, at injection site; headache, abdominal
obtunded pts, air-filled syringe may be cramps, vulvular pain, flushed skin, mild
attached to catheter to deposit solution. B/P elevation, nausea with high dosages.
Nasal: Rhinorrhea, nasal congestion,
INDICATIONS/ROUTES/DOSAGE slight B/P elevation.
Primary Nocturnal Enuresis ADVERSE EFFECTS/TOXIC
PO: CHILDREN 6 YRS AND OLDER: 0.2–0.6 REACTIONS
mg once before bedtime. Limit fluid intake
Water intoxication, hyponatremia (head-
1 hr prior and at least 8 hrs after dose.
ache, drowsiness, confusion, decreased
Central Cranial Diabetes Insipidus urination, rapid weight gain, seizures,
b ALERT c Fluid restriction should be coma) may occur in overhydration. Chil-
observed. dren, elderly pts, infants are esp. at risk.
PO: ADULTS, ELDERLY, CHILDREN 4 YRS
AND OLDER: Initially, 0.05 mg twice daily. NURSING CONSIDERATIONS
Titrate to desired response. Range: 0.1– BASELINE ASSESSMENT
1.2 mg/day in 2–3 divided doses.
Establish baselines for B/P, pulse, weight,
IV, SQ: ADULTS, ELDERLY, CHILDREN
serum electrolytes, urine specific gravity.
12 YRS AND OLDER: 2–4 mcg/day in 2
Check lab values for factor VIII coagulant
divided doses or one-tenth of mainte-
concentration for hemophilia A, von Wil-
nance intranasal dose.
lebrand’s disease; bleeding times.
Intranasal: (Use 100 mcg/mL Con-
centration): ADULTS, ELDERLY, CHILDREN INTERVENTION/EVALUATION
OLDER THAN 12 YRS: 10–40 mcg (0.1– Check B/P, pulse with IV infusion. Moni-
0.4 mL) in 1–3 doses/day. Usual dose: tor pt weight, fluid intake; urine volume,
10 mcg 2 times/day. CHILDREN 3 MOS–12 urine specific gravity, osmolality, serum
underlined – top prescribed drug
dexamethasone 325
electrolytes for diabetes insipidus. Assess Cautions: Thyroid disease, renal/hepatic
factor VIII antigen levels, aPTT, factor VIII impairment, cardiovascular disease, diabe-
activity level for hemophilia. tes, glaucoma, cataracts, myasthenia gravis,
pts at risk for seizures, osteoporosis, post-
PATIENT/FAMILY TEACHING
MI, elderly.
• Avoid overhydration. • Follow guide- D
lines for proper intranasal administra- ACTION
tion. • Report headache, shortness of Decreases inflammation by suppres-
breath, heartburn, nausea, abdominal sion of neutrophil migration, de­creases
cramps. production of inflammatory mediators.
Reverses increased capillary perme-
ability. Suppresses normal immune
dexamethasone response. Therapeutic Effect:
Decreases inflammation.
dex-a-meth-a-sone
(Decadron, Dexamethasone Inten- PHARMACOKINETICS
sol, DexPak, Maxidex) Rapidly absorbed from GI tract after
Do not confuse Decadron with PO administration. Widely distributed.
Percodan, or dexamethasone Protein binding: High. Metabolized in
with dextroamphetamine, or liver. Primarily excreted in urine. Mini-
Maxidex with Maxzide. mally removed by hemodialysis. Half-
life: 3–4.5 hrs.
FIXED-COMBINATION(S)
Ciprodex Otic: dexamethasone/cip- LIFESPAN CONSIDERATIONS
rofloxacin (antibiotic): 0.1%/0.3%. Pregnancy/Lactation: Crosses pla-
Dexacidin, Maxitrol: dexametha- centa. Distributed in breast milk. Children:
sone/neomycin/polymyxin (anti-in- Prolonged treatment with high-dose ther­
fectives): 0.1%/3.5 mg/10,000 units apy may decrease short-term growth
per g or mL. rate, cortisol secretion. Elderly: Higher
risk for developing hypertension,
uCLASSIFICATION osteoporosis.
PHARMACOTHERAPEUTIC: Gluco-
corticoid. CLINICAL: Anti-inflamma- INTERACTIONS
tory. Antiemetic. DRUG: Amphotericin may increase
hy­pokalemia. CYP3A4 inducers
(e.g., carBAMazepine, phenytoin,
USES rifAMPin) may decrease concentration.
Used primarily as an anti-inflammatory or CYP3A4 inhibitors (e.g., clarithro-
immunosuppressant agent in a variety of mycin, ketoconazole, ritonavir),
diseases (e.g., allergic states, edematous macrolide antibiotics may increase
states, neoplastic diseases, rheumatic concentration. May decrease therapeu-
disorders). OFF-LABEL: Antiemetic, treat- tic effect of aldesleukin. May increase
ment of croup, dexamethasone suppres- hyponatremic effect of desmopressin.
sion test (indicator consistent with suicide Live virus vaccines may decrease pt’s
and/or depression), accelerate fetal lung antibody response to vaccine, increase
maturation. Treatment of acute mountain vaccine side effects, potentiate virus
sickness, high-altitude cerebral edema. replication. HERBAL: Echinacea may
increase immunosuppressant effect. St.
PRECAUTIONS John’s wort may decrease concentra-
Hypersensitivity to dexa­
Contraindications: tion/effect. FOOD: Interferes with cal-
methasone. Systemic fungal infections. cium absorption. LAB VALUES: May

Canadian trade name Non-Crushable Drug High Alert drug


326 dexamethasone
increase serum glucose, lipids, sodium IV COMPATIBILITIES
levels. May decrease serum calcium, Cimetidine (Tagamet), CISplatin (Plati-
potassium, thyroxine, WBC. nol), cyclophosphamide (Cytoxan), cyta-
rabine (Cytosar), DOCEtaxel (Taxotere),
AVAILABILITY (Rx)
DOXOrubicin (Adriamycin), etoposide
D Elixir: 0.5 mg/5 mL. Injection, Solu- (VePesid), furosemide (Lasix), granis-
tion: 4 mg/mL, 10 mg/mL. Ophthalmic etron (Kytril), heparin, HYDROmorphone
Solution: 0.1%. Ophthalmic Suspension: (Dilaudid), LORazepam (Ativan), mor-
0.1%. Solution, Oral: 0.5 mg/5 mL. Solu- phine, ondansetron (Zofran), PACLitaxel
tion, Oral Concentrate: (Dexamethasone (Taxol), palonosetron (Aloxi), potassium
Intensol): 1 mg/mL. Tablets: 0.5 mg, chloride, propofol (Diprivan).
0.75 mg, 1 mg, 1.5 mg, 2 mg, 4 mg, 6 mg.
INDICATIONS/ROUTES/DOSAGE
ADMINISTRATION/HANDLING
Anti-Inflammatory
IV PO, IV, IM: ADULTS, ELDERLY: 0.5–9
mg/day in divided doses q6–12h. CHIL-
b ALERT c Dexamethasone sodium DREN: 0.02–0.3 mg/kg/day in divided
phosphate may be given by IV push or IV doses q6–12h. Intra-articular: ADULTS,
infusion. Rapid injection may cause geni- ELDERLY: 0.4–6 mg/day.
tal burning sensation in females.
• For IV push, give over 1–4 min if dose Cerebral Edema
is less than 10 mg. • For IV infusion, mix IV: ADULTS, ELDERLY: Initially, 10 mg,
with 50–100 mL 0.9% NaCl or D5W and then 4 mg (IV or IM) q6h.
infuse over 15–30 min. • For neonates, PO, IV, IM: CHILDREN: Loading dose
solution must be preservative free. • IV of 1–2 mg/kg, then 1–1.5 mg/kg/day in
solution must be used within 24 hrs. divided doses q4–6h.
IM Nausea/Vomiting in Chemotherapy Pts
• Give deep IM, preferably in gluteus Note: Refer to individual protocols and
maximus. emetogenic potential.
IV: ADULTS, ELDERLY: 8–20 mg 15–30
PO min before treatment. CHILDREN: 2 mg
• Give with milk, food (to decrease GI q12h up to 6 mg/m2/dose q6h.
effect).
Usual Ophthalmic Dosage, Ocular
Ophthalmic Solution, Suspension Inflammatory Conditions
• Place gloved finger on lower eyelid and ADULTS, ELDERLY, CHILDREN: (Solution):
pull out until a pocket is formed between Initially, 2 drops q1h while awake and
eye and lower lid. • Place prescribed q2h at night for 1 day, then reduce to 3–4
number of drops or 14–12 inch ointment times/day. (Suspension): 1–2 drops up to
into pocket. • Instruct pt to close eye 4–6 times/day.
gently for 1–2 min (so that medication will
not be squeezed out of the sac). • Instruct Dosage in Renal/Hepatic Impairment
pt to apply digital pressure to lacrimal sac No dose adjustment.
at inner canthus for 1–2 min to minimize
systemic absorption. SIDE EFFECTS
Frequent: Inhalation: Cough, dry mouth,
IV INCOMPATIBILITIES hoarseness, throat irritation. Intranasal:
Ciprofloxacin (Cipro), DAUNOrubicin Burning, mucosal dryness. Ophthalmic:
(Cerubidine), IDArubicin (Idamycin), Blurred vision. Systemic: Insomnia,
midazolam (Versed). facial edema (cushingoid appearance

underlined – top prescribed drug


dexmedetomidine 327
[“moon face”]), moderate abdominal serum electrolytes, esp. for hypercal-
distention, indigestion, increased appe- cemia, hypokalemia, paresthesia (esp.
tite, nervousness, facial flushing, diapho- lower extremities, nausea/vomiting, ir-
resis. Occasional: Inhalation: Localized ritability), Hgb, occult blood loss. Assess
fungal infection (thrush). Intranasal: emotional status, ability to sleep. Abrupt
Crusting inside nose, epistaxis, sore withdrawal may cause adrenal insuffi- D
throat, ulceration of nasal mucosa. ciency; taper dose gradually.
Ophthalmic: Decreased vision; lacrima-
PATIENT/FAMILY TEACHING
tion; eye pain; burning, stinging, redness
of eyes; nausea; vomiting. Systemic: • Do not change dose/schedule or stop
Dizziness, decreased/blurred vision. taking drug. • Must taper off gradually
Rare: Inhalation: Increased broncho- under medical supervision. • Report
spasm, esophageal candidiasis. Intra- fever, sore throat, muscle aches, sudden
nasal: Nasal/pharyngeal candidiasis, weight gain, edema, exposure to measles/
eye pain. Systemic: Generalized allergic chickenpox. • Severe stress (serious
reaction (rash, urticaria); pain, redness, infection, surgery, trauma) may require
swelling at injection site; psychological increased dosage. • Inform dentist,
changes; false sense of well-being; hallu- other physicians of dexamethasone ther-
cinations; depression. apy within past 12 mos. • Avoid alco-
hol, limit caffeine.
ADVERSE EFFECTS/TOXIC
REACTIONS
Long-term therapy: Muscle wasting
(esp. arms, legs), osteoporosis, sponta- dexmedetomidine
neous fractures, amenorrhea, cataracts,
glaucoma, peptic ulcer disease, HF. dex-med-e-toe-mye-deen
Ophthalmic: Glaucoma, ocular hyper- (Precedex)
tension, cataracts. Abrupt withdrawal Do not confuse Precedex with
following long-term therapy: Severe Percocet or Peridex.
joint pain, severe headache, anorexia,
uCLASSIFICATION
nausea, fever, rebound inflammation,
fatigue, weakness, lethargy, dizziness, PHARMACOTHERAPEUTIC: Alpha 2
orthostatic hypotension. agonist. CLINICAL: Sedative.

NURSING CONSIDERATIONS
USES
BASELINE ASSESSMENT Sedation of initially intubated, mechanically
Question for hypersensitivity to any cor- ventilated adults in intensive care setting.
ticosteroids. Obtain baselines for height, Use in nonintubated pts requiring sedation
weight, B/P, serum glucose, electro- before and/or during surgical and other
lytes. Question medical history as listed procedures. OFF-LABEL: Treatment of shiv-
in Precautions. ering, use in children. Awake craniotomy.
INTERVENTION/EVALUATION PRECAUTIONS
Monitor I&O, daily weight, serum glu- Contraindications: Hypersensitivity to dex-
cose. Assess for edema. Evaluate food medetomidine. Cautions: Heart block,
tolerance. Monitor daily pattern of bowel bradycardia, hepatic impairment, hypo-
activity, stool consistency. Report hyper- volemia, diabetes, hypotension, chronic
acidity promptly. Check vital signs at least hypertension, severe ventricular dysfunc-
twice daily. Be alert to infection (sore tion, elderly, use of vasodilators or drugs
throat, fever, vague symptoms). Monitor decreasing heart rate.

Canadian trade name Non-Crushable Drug High Alert drug


328 dexmedetomidine

ACTION with 48 mL 0.9% NaCl for a final concen-


Selective alpha2-adrenergic agonist. Inhib- tration of 4 mcg/mL.
its norepinephrine release. Therapeutic Rate of administration • Individual-
Effect: Produces anesthetic, sedative ized, titrated to desired effect. Use con-
effects. trolled infusion pump.
D Storage • Store at room temperature.
PHARMACOKINETICS
IV INCOMPATIBILITIES
Protein binding: 94%. Metabolized in
liver. Excreted in urine (85%), feces Do not mix with any other medications.
(4%). Half-life: 2 hrs.
IV COMPATIBILITIES
LIFESPAN CONSIDERATIONS Amiodarone (Cordarone), bumetanide
Pregnancy/Lactation: Unknown if dis- (Bumex), calcium gluconate, cisatracu-
tributed in breast milk. Children: Safety rium (Nimbex), dexamethasone, DOBU-
and efficacy not established. Elderly: Tamine, DOPamine, magnesium sulfate,
May have increased risk of hypotension. norepinephrine (Levophed), propofol
(Diprivan).
INTERACTIONS
INDICATIONS/ROUTES/
DRUG: Sedatives (e.g., midazolam,
DOSAGE
LORazepam), opioids (e.g., fen-
taNYL, morphine, HYDROmor- ICU Sedation
phone), hypnotics (e.g., zolpidem, IV: ADULTS: Loading dose of 1 mcg/
temazepam) may increase CNS depres- kg over 10 min followed by mainte-
sion. Antihypertensives (e.g., amLO- nance infusion of 0.2–0.7 mcg/kg/
DIPine, cloNIDine, lisinopril, hr. ELDERLY: May require decreased
valsartan) may increase risk of hypoten- dosage.
sion. Beta blockers (e.g., carvedilol,
Dosage in Renal Impairment
metoprolol), calcium channel block-
ers (e.g., dilTIAZem, verapamil) may No dose adjustment.
increase risk of bradycardia, hypoten-
Dosage in Hepatic Impairment
sion. Tricyclic antidepressants (e.g.,
Use caution.
amitriptyline, doxepin) may decrease
antihypertensive effect. HERBAL: None SIDE EFFECTS
significant. FOOD: None known. LAB
Frequent (25%–12%): Hypotension, hyper-
VALUES: May increase serum alkaline
phosphatase, ALT, AST, glucose, potas- tension. Occasional (9%–3%): Nausea,
sium. May decrease serum calcium, mag- constipation, bradycardia, pyrexia, dry
nesium; Hgb, Hct, RBC. mouth, vomiting, hypovolemia. Rare (2%–
less than 1%): Agitation, hyperpyrexia,
AVAILABILITY (Rx) thirst, oliguria, wheezing.
Injection Solution:80 mcg/20 mL, 200 ADVERSE EFFECTS/TOXIC
mcg/2 mL vials, 4 mcg/mL solutions (50 REACTIONS
mL, 100 mL).
Significant bradycardia, sinus arrest,
ADMINISTRATION/HANDLING cardiac arrest, AV block, SVT, ventricular
tachycardia may occur and may be fatal.
IV Transient hypertension was reported
Reconstitution • Visually inspect for during loading doses. Atrial fibrillation,
particulate matter or discoloration. Solu- hypoxia, pleural effusion may occur
tion should appear clear, color- with too-rapid IV infusion. Bradycardia,
less. • Dilute 2 mL of dexmedetomidine hypotension may be more pronounced

underlined – top prescribed drug


dextroamphetamine and amphetamine 329
in pts with diabetes, hypovolemia, Do not confuse Adderall with
hypertension, or who are elderly. Acute Inderal.
respiratory distress syndrome (ARDS),
respiratory failure, acidosis may occur uCLASSIFICATION
with prolonged infusion time greater PHARMACOTHERAPEUTIC: Amphet-
than 24 hrs. amine (Schedule II). CLINICAL: CNS D
stimulant.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT USES
Obtain baseline B/P, heart rate. Recommend Treatment of narcolepsy (immediate-
continuous cardiac monitoring during use. release only); treatment of ADHD.
Assess mental status prior to initiation.
Obtain full medication history; screen for PRECAUTIONS
medications known to cause hypotension, Contraindications: Hypersensitivity to
bradycardia, sedation. Question history of dextroamphetamine, amphetamine, or
heart block, bradycardia, severe ventricular sympathomimetics. Advanced arterio-
dysfunction; hepatic impairment. sclerosis, agitated mental states, glau-
INTERVENTION/EVALUATION coma, history of alcohol or drug abuse,
Assess cardiac monitor for arrhythmia, hypersensitivity to sympathomimetic
bradycardia, hypotension. Anticholiner- amines, hyperthyroidism, moderate to
gic agents (e.g., glycopyrrolate, atropine) severe hypertension, symptomatic car-
may be effective in treating drug-induced diovascular disease, use of MAOIs within
bradycardia. Monitor level of sedation; re- 14 days. Cautions: Elderly, debilitated
spiratory rate, rhythm. Monitor ventilator pts, history of seizures, mild hyperten-
settings. Discontinue once pt is extubated. sion. Preexisting psychotic or bipolar
disorder.
PATIENT/FAMILY TEACHING
• B/P, heart will be continuously moni- ACTION
tored during infusion. • If infusion is Promotes release of primarily dopamine
used for more than 6 hrs, agitation, ner- and norepinephrine from storage site
vousness, headaches may occur for up to in presynaptic nerve terminals. Thera-
48 hrs. • Report other symptoms that peutic Effect: Increases motor activity,
may occur within 48 hrs (abdominal mental alertness; decreases drowsiness,
pain, confusion, constipation, dizziness, fatigue; suppresses appetite.
sweating, weakness, salt cravings, weight
loss). PHARMACOKINETICS
Well absorbed following PO adminis-
tration. Widely distributed including
dextroamphetamine CNS. Metabolized in liver. Excreted in
urine. Removed by hemodialysis. Half-
and amphetamine life: 10–13 hrs.

dex-troe-am-fet-ah-meen/am-fet- LIFESPAN CONSIDERATIONS


ah-meen Pregnancy/Lactation: Distributed in
(Adderall, Adderall-XR, Mydayis) breast milk. Children: Safety and effi-
j BLACK BOX ALERT jHigh cacy not established in pts younger than
potential for abuse. Prolonged 3 yrs. Elderly: Age-related cardiovas-
administration may lead to drug de- cular, cerebrovascular disease, hepatic/
pendence. Severe cardiovascular renal impairment may increase risk of
events including CVA/MI reported.
side effects.

Canadian trade name Non-Crushable Drug High Alert drug


330 dextroamphetamine and amphetamine

INTERACTIONS DREN 13–17 YRS: (Adderall): Initially, 5 mg


DRUG: MAOIs (e.g., phenelzine, 1–2 times/day. May increase by 5 mg at
selegiline) may ­ prolong, intensify wkly intervals. Maximum: 40 mg/day
effects. HERBAL: None significant. in 1–3 divided doses (usual intervals of
FOOD: None known. LAB VALUES: May 4–6 hrs). (Adderall-XR): Initially, 10 mg
D increase plasma corticosteroid. once daily in the morning. May increase
to 20 mg/day after 1 wk if symptoms are
AVAILABILITY (Rx) not controlled. May increase up to 60 mg/
5 mg, 7.5 mg, 10 mg,
Tablets: (Adderall): day. (Mydayis): Initially, 12.5 mg once
12.5 mg, 15 mg, 20 mg, 30 mg. daily in morning. May increase by 12.5
mg no sooner than once wkly. Maxi-
Capsules: (Extended-Release [Adder- mum: 25 mg/day. CHILDREN 6–12 YRS:
all-XR]): 5 mg, 10 mg, 15 mg, 20 mg, 25 (Adderall): Initially, 5 mg 1–2 times/day.
mg, 30 mg. Mydayis: 12.5 mg, 25 mg, May increase in 5-mg increments at wkly
37.5 mg, 50 mg. intervals until optimal response is ob-
ADMINISTRATION/HANDLING tained. Maximum: 40 mg/day given in
1–3 divided doses (use intervals of 4–6
PO hrs between additional doses). (Adderall-
• Give immediate-release tablets at least XR): Initially, 5–10 mg once daily in the
6 hrs before bedtime to prevent insom- morning. May increase daily dose in 5- to
nia. • Extended-release capsules should 10-mg increments at wkly intervals. Maxi-
be swallowed whole; do not break, crush, mum: 30 mg/day. CHILDREN 3–5 YRS: (Ad-
or cut. • Avoid afternoon doses to pre- derall): Initially, 2.5 mg/day given every
vent insomnia. • May open capsules and morning. May increase daily dose in 2.5-
sprinkle on applesauce. Instruct pt not to mg increments at wkly intervals until opti-
chew sprinkled beads; take immediately. mal response is obtained. Maximum: 40
INDICATIONS/ROUTES/DOSAGE mg/day given in 1–3 divided doses (use
intervals of 4–6 hrs between additional
Narcolepsy doses). Not recommended in children
PO: ADULTS, CHILDREN OLDER THAN 12 younger than 3 yrs.
YRS: Initially, 10 mg/day. Increase by 10
mg/day at wkly intervals until therapeutic Dosage in Renal/Hepatic Impairment
response is achieved. Usual Range: 5–60 No dose adjustment.
mg/day given in 1–3 divided doses.
CHILDREN 6–12 YRS: Initially, 5 mg/day. SIDE EFFECTS
Increase by 5 mg/day at wkly intervals until Frequent: Increased motor activ-
therapeutic response is achieved. Usual ity, talk­ativeness, nervousness, mild
Range:  5–60 mg/day given in 1–3 divided euphoria, insomnia. Occasional: Head-
doses ache, chills, dry mouth, GI distress,
worsening depression in pts who are
ADHD clinically depressed, tachycardia, palpi-
ADULTS, ELDERLY: (Adderall): Initially, 5 mg tations, chest pain, dizziness, decreased
1–2 times/day. May increase by 5-mg in- appetite.
crements at wkly intervals. Maximum: 40
mg/day in 1–3 divided doses (usual inter- ADVERSE EFFECTS/TOXIC
vals of 4–6 hrs). (Adderall-XR): Initially, REACTIONS
20 mg once daily in the morning. May Overdose may produce skin pallor/flush-
increase up to 60 mg/day. (Mydayis): Ini- ing, arrhythmias, psychosis. Abrupt with-
tially, 12.5–25 mg once daily in morning. drawal after prolonged use of high doses
May increase by 12.5 mg no sooner than may produce lethargy (may last for wks).
once wkly. Maximum: 50 mg/day.  CHIL- Prolonged administration to children

underlined – top prescribed drug


diazePAM 331
with ADHD may temporarily suppress USES
normal weight/height pattern. Short-term relief of anxiety symptoms,
relief of acute alcohol withdrawal.
NURSING CONSIDERATIONS
Adjunct for relief of acute musculoskel-
BASELINE ASSESSMENT etal conditions, treatment of seizures
(IV route used for termination of status D
Assess attention span, impulse control,
interaction with others. Screen for drug- epilepticus). Gel: Control of increased
seeking behavior, past drug abuse. Ob- seizure activity in refractory epilepsy
tain baseline B/P. Assess sleep pattern. in pts on stable regimens. OFF-LABEL:
Treatment of panic disorder. Short-term
INTERVENTION/EVALUATION treatment of spasticity in children with
Monitor for CNS overstimulation, in- cerebral palsy. Sedation for mechanically
crease in B/P, growth rate, change in vented pts in ICU.
pulse rate, respirations, weight loss. Nar-
colepsy: Observe/document frequency PRECAUTIONS
of narcoleptic episodes. ADHD: Observe Contraindications:Hypersensitivity to diaz­
for improved attention span. epam. Acute narrow-angle glaucoma,
untreated open-angle glaucoma, severe
PATIENT/FAMILY TEACHING
respiratory depression, severe hepatic
• Normal dosage levels may produce tol- insufficiency, sleep apnea syndrome,
erance to drug’s anorexic mood-elevating myasthenia gravis. Children younger than
effects within a few wks. • Dry mouth 6 mos (oral). Cautions: Pts receiving
may be relieved with sugarless gum, sips other CNS depressants or psychoactive
of water. • Take early in day. • Do agents, depression, history of drug and
not break, chew, or crush extended-re- alcohol abuse, renal/hepatic impairment,
lease capsules. • May mask extreme fa- respiratory disease, impaired gag reflex,
tigue. • Report pronounced anxiety, concurrent use of strong CYP3A4 inhibi-
dizziness, decreased appetite, dry mouth, tors or inducers.
new or worsening behavior, chest pain,
palpitations. • Avoid alcohol, caffeine. ACTION
Depresses all levels of CNS by enhanc-
ing action of gamma-aminobutyric
acid (GABA), a major inhibitory neu-
rotransmitter in the brain. Therapeu-
diazePAM tic Effect: Produces anxiolytic effect,
elevates seizure threshold, produces
dye-az-e-pam skeletal muscle relaxation.
(Apo-Diazepam , Diastat, Diaz-
ePAM Intensol, Novo-Dipam ,
PHARMACOKINETICS
Valium) Well absorbed from GI tract. Widely dis-
Do not confuse diazePAM with tributed. Protein binding: 98%. Excreted
diazoxide, dilTIAZem, Ditropan, in urine. Minimally removed by hemodi-
or LORazepam, or Valium with alysis. Half-life: 20–70 hrs (increased
Valcyte. in hepatic dysfunction, elderly).

uCLASSIFICATION LIFESPAN CONSIDERATIONS


PHARMACOTHERAPEUTIC: Ben- Pregnancy/Lactation: Crosses plac­e­nta.
zodiazepine (Schedule IV). CLINI- Distributed in breast milk. May increase
CAL: Antianxiety, skeletal muscle risk of fetal abnormalities if administered
relaxant, anticonvulsant. during first trimester of pregnancy. Chronic
ingestion during pregnancy may produce
Canadian trade name Non-Crushable Drug High Alert drug
332 diazePAM
withdrawal symptoms, CNS depression in IM
neonates. Children/Elderly: Use small • Injection may be painful. Inject deeply
initial doses with gradual increases to into large muscle mass.
avoid ataxia, excessive sedation. Elderly at PO
increased risk of impaired cognition, delir- • Give without regard to food. • Dilute
D ium, falls, fractures. oral concentrate with water, juice, carbon-
INTERACTIONS ated beverages; may be mixed in semisolid
food (applesauce, pudding). • Tablets
DRUG: Alcohol, CNS depressants may be crushed.
(e.g., gabapentin, morphine, zol-
pidem) may increase CNS depression. GEL
CYP3A4 inducers (e.g., carBAMaze- • Insert rectal tip and gently push
pine, rifAMPin) may decrease con- plunger over 3 sec. Remove tip after 3
centration. CYP3A4 inhibitors (e.g., additional sec. • Buttocks should be
itraconazole, ketoconazole) may held together for 3 sec after removal.
increase concentration/effect. OLAN- IV INCOMPATIBILITIES
Zapine may increase adverse effects.
HERBAL: Herbals with sedative prop- Amphotericin B complex (Abelcet, AmBi-
erties (e.g., chamomile, kava kava, some, Amphotec), cefepime (Maxipime),
valerian) may increase CNS depres- dilTIAZem (Cardizem), fluconazole (Diflu-
sion. St. John’s wort may decrease can), foscarnet (Foscavir), furosemide
concentration/effects. FOOD: Grapefruit (Lasix), heparin, hydrocortisone (SOLU-
products may increase concentration/ Cortef), HYDROmorphone (Dilaudid),
effects. LAB VALUES: None significant. meropenem (Merrem IV), potassium
Therapeutic serum level: 0.5–2 mcg/ chloride, propofol (Diprivan), vitamins.
mL; toxic serum level: greater than 3 IV COMPATIBILITIES
mcg/mL.
DOBUTamine (Dobutrex), fentaNYL, mor­
AVAILABILITY (Rx) phine.
Injection, Solution: 5 mg/mL. Oral Con- INDICATIONS/ROUTES/DOSAGE
centrate: (DiazePAM Intensol): 5 mg/mL.
Anxiety
Oral Solution: 5 mg/5 mL. Rectal Gel:
PO: ADULTS: 2–10 mg 2–4 times/day.
(Diastat): 2.5 mg, 10 mg, 20 mg. Tablet:
ELDERLY: Initially, 1–2 mg 1–2
times/day.
(Valium): 2 mg, 5 mg, 10 mg.
CHILDREN: 0.12–0.8 mg/kg/day
in divided
ADMINISTRATION/HANDLING doses q6–8h.
IV, IM: ADULTS: 2–10 mg; may repeat in
IV 3–4 hrs if needed.
Rate of administration • Give by IV Skeletal Muscle Relaxation
push into tubing of flowing IV solution as PO: ADULTS: 2–10 mg 2–4 times/day.
close as possible to vein insertion ELDERLY: Initially, 1–2 mg 1–2 times/
point. • Administer directly into large vein day. CHILDREN: 0.12–0.8 mg/kg/day in
(reduces risk of thrombosis/phlebitis). Do divided doses q6–8h.
not use small veins (e.g., wrist/dorsum of Seizures
hand). • Administer IV at rate not exceed- PO: ADULTS, ELDERLY: (Adjunctive):
ing 5 mg/min for adults. For children, give 2–10 mg 2–4 times/day.
1–2 mg/min (too-rapid IV may result in Muscle spasms
hypotension, respiratory depression). PO: ADULTS, ELDERLY: 2–10 mg 3–4
• Monitor respirations q5–15 min for times/day.
2 hrs. IV/IM: Initially, 5–10 mg, then 5–10 mg
Storage • Store at room temperature. in 3–4 hrs if needed.
underlined – top prescribed drug
diazePAM 333
Alcohol Withdrawal syndrome. Abrupt or too-rapid with-
IM, IV: ADULTS, ELDERLY: Initially, 10 drawal may result in pronounced rest-
mg, then 5–10 mg 3–4 hrs later. PO: lessness, irritability, insomnia, hand
ADULTS, ELDERLY: 10 mg 3–4 times dur- tremor, abdominal/muscle cramps,
ing first 24 hrs, then reduce to 5 mg 3–4 diaphoresis, vomiting, seizures. Abrupt
times/day as needed. withdrawal in pts with epilepsy may D
produce increase in frequency/sever-
Status Epilepticus ity of seizures. Overdose results in
IV: ADULTS, ELDERLY: 0.15–0.2 mg/kg. drowsiness, confusion, diminished
Maximum: 10 mg. May repeat once. reflexes, CNS depression, coma. Anti-
INFANTS, CHILDREN: 0.1–0.3 mg/kg over dote: Flumazenil (see Appendix J for
2 min; may repeat after 5–10 min. Maxi- dosage).
mum: 10 mg/dose.
NURSING CONSIDERATIONS
Control of Increased Seizure Activity
(Breakthrough Seizures) in Pts with BASELINE ASSESSMENT
Refractory Epilepsy Who Are on Stable Assess B/P, pulse, respirations imme-
Regimens of Anticonvulsants diately before administration. Anxi-
Note: Do not use gel for more than 5 ety: Assess autonomic response (cold,
episodes/mo or more than 1 episode clammy hands; diaphoresis), motor
q5days. response (agitation, trembling, ten-
PO: ADULTS, ELDERLY: 2–10 mg 2–4 sion). Musculoskeletal spasm: Re-
times/day. cord onset, type, location, duration of
Rectal gel: ADULTS, CHILDREN 12 YRS AND pain. Check for immobility, stiffness,
OLDER: 0.2 mg/kg; may be repeated in 4–12 swelling. Seizures: Review history
hrs. CHILDREN 6–11 YRS: 0.3 mg/kg; may of seizure disorder (length, intensity,
be repeated in 4–12 hrs. Maximum: 20 frequency, duration, LOC). Observe
mg. CHILDREN 2–5 YRS: 0.5 mg/kg; may be frequently for recurrence of seizure
repeated in 4–12 hrs. Maximum: 20 mg. activity.
Dosage in Renal Impairment INTERVENTION/EVALUATION
Use caution. Monitor heart rate, respiratory rate,
B/P, mental status. Assess children,
Dosage in Hepatic Impairment elderly for paradoxical reaction, par-
Use caution. Oral tablets contraindicated ticularly during early therapy. Evaluate
in severe hepatic impairment. for therapeutic response (decrease in
intensity/frequency of seizures; calm fa-
SIDE EFFECTS cial expression, decreased restlessness;
Frequent: Pain with IM injection, drowsiness, decreased intensity of skeletal muscle
fatigue, ataxia. Occasional: Slurred speech, pain). Therapeutic serum level:
orthostatic hypotension, headache, hypoac- 0.5–2 mcg/mL; toxic serum level:
tivity, constipation, nausea, blurred vision. greater than 3 mcg/mL.
Rare: Paradoxical CNS reactions (hyperactiv-
ity/nervousness in children, excitement/rest- PATIENT/FAMILY TEACHING
lessness in elderly/debilitated pts) generally • Avoid alcohol. • Limit caffeine. •
noted during first 2 wks of therapy, particu- May cause drowsiness; avoid tasks that re-
larly in presence of uncontrolled pain. quire alertness, motor skills until response
to drug is established. • May be habit
ADVERSE EFFECTS/TOXIC forming. • Avoid abrupt discontinuation
REACTIONS after prolonged use.
IV route may produce pain, swell-
ing, thrombophlebitis, carpal tunnel
Canadian trade name Non-Crushable Drug High Alert drug
334 diclofenac

PRECAUTIONS
diclofenac Contraindications: Hypersensitivity to diclo­
fenac. Pts experiencing asthma, urticaria
dye-kloe-fen-ak
after taking aspirin, other NSAIDs. Pts with
(Cambia, Flector, Voltaren Gel,
moderate to severe renal impairment in
D Zipsor, Zorvolex)
perioperative period who are at risk for
j BLACK BOX ALERT j Increased volume depletion (injection only); peri-
risk of serious cardiovascular
thrombotic events, including myo- operative pain in setting of CABG surgery.
cardial infarction, CVA. Increased Cautions: HF, hypertension, renal/hepatic
risk of severe GI reactions, includ- impairment, hepatic porphyria, history of GI
ing ulceration, bleeding, perforation disease (e.g., bleeding, ulcers), concomi-
of stomach, intestines. Contraindi- tant use of aspirin or anticoagulants, elderly,
cated for treatment of perioperative
pain in setting of CABG surgery. debilitated pts.
Do not confuse Cataflam with
Catapres, diclofenac with Diflu-
ACTION
can or Duphalac, or Voltaren with Reversibly inhibits cyclo-oxygenase-1
traMADol, Ultram, or Verelan. and -2 (COX-1 and COX-2) enzymes,
resulting in decreased formation of
FIXED-COMBINATION(S) prostaglandin precursors. Therapeutic
Arthrotec: diclofenac/miSOPROS- Effect: Produces analgesic, antipyretic,
tol (an antisecretory gastric protec- anti-inflammatory effects.
tant): 50 mg/200 mcg, 75 mg/200
mcg.
PHARMACOKINETICS
Route Onset Peak Duration
uCLASSIFICATION PO 30 min 2–3 hrs Up to 8 hrs
PHARMACOTHERAPEUTIC: NSAID
(nonselective). CLINICAL: Analgesic, Completely absorbed from GI tract. Pro-
anti-inflammatory. tein binding: greater than 99%. Widely
distributed. Metabolized in liver. Primar-
ily excreted in urine. Minimally removed
USES by hemodialysis. Half-life: 1.2–2 hrs.
PO: (Immediate-Release): Treat- LIFESPAN CONSIDERATIONS
ment of rheumatoid arthritis, osteoar-
thritis, mild to moderate acute pain, Pregnancy/Lactation: Crosses pla-
primary dysmenorrhea. (Zipsor): Mild centa. Unknown if distributed in breast
to moderate pain. (Zorvolex): Mild milk. Avoid use during third trimester
to moderate pain, osteoarthritic pain. (may adversely affect fetal cardiovascular
(Delayed-Release): Treatment of rheu- system: premature closure of ductus arte-
matoid arthritis, osteoarthritis, ankylos- riosus). Children: Safety and efficacy
ing spondylitis. (Extended-Release): not established. Elderly: GI bleeding,
Treatment of rheumatoid arthritis, ulceration more likely to cause serious
osteoarthritis. Oral Solution (Cam- adverse effects. Age-related renal impair-
bia): Treatment of migraine. Powder ment may increase risk of hepatic/renal
for Oral Solution: Acute treatment of toxicity; reduced dosage recommended.
migraine attacks with or without aura. INTERACTIONS
Topical Patch: Treatment of acute pain
due to minor strains, sprains, contu- DRUG: Aspirin, NSAIDs (e.g.,
sions. OFF-LABEL: Treatment of juvenile ibuprofen, naproxen) may
idiopathic arthritis. increase risk of GI side effects/bleed-
ing. May increase cycloSPORINE

underlined – top prescribed drug


diclofenac 335
concentration/toxicity. HERBAL: Herb- PO: (Extended-Release): ADULTS,
als with anticoagulant/antiplatelet ELDERLY: 100 mg once daily. May increase
activity (e.g., garlic, ginger, ginkgo to 200 mg/day in 2 divided doses.
biloba) may increase adverse effects. PO: (Delayed-Release): ADULTS,
FOOD: None known. LAB VALUES: May ELDERLY: 50 mg 3–4 times/day or 75 mg
increase urine protein, serum BUN, twice daily. D
alkaline phosphatase, creatinine, LDH,
potassium, ALT, AST. May decrease Ankylosing Spondylitis
serum uric acid. PO: (Delayed-Release): ADULTS, ELDERLY:
100–125 mg/day in 4–5 divided doses.
AVAILABILITY (Rx)
Primary Dysmenorrhea
Transdermal Patch: (Flector): 1.3%. Trans-
PO: (Immediate-Release): ADULTS,
dermal Gel: (Voltaren): 1%. Capsules:
ELDERLY: 50 mg 3 times/day.
(Zipsor): 25 mg. (Zorvolex): 18 mg,
35 mg. Oral Solution: (Cambia): 50-mg Pain
packets. Tablets: 50 mg. PO: ADULTS, ELDERLY: (Immediate-
Tablets: (Delayed-Release): 25 mg, Release): 100 mg once, then 50 mg 3
50 mg, 75 mg. Tablets: (Extended- times/day. (Zipsor): 25 mg 4 times/day.
Release): 100 mg. (Zorvolex): 18–35 mg 3 times/day.
IV: 37.5 mg q6h prn. Maximum: 150
ADMINISTRATION/HANDLING mg/day.
PO Topical Patch: (Flector): Apply 2 times/day.
• Do not break, crush, dissolve, or
divide enteric-coated tablets. • May Migraine (Oral Solution)
give with food, milk, antacids if GI dis- PO: ADULTS, ELDERLY: 50 mg (one
tress occurs. • (Cambia): Mix one packet) once.
packet in 1–2 oz water, stir well, and Dosage in Renal Impairment
instruct pt to drink immediately. Not recommended in severe impairment.
Transdermal Patch Dosage in Hepatic Impairment
• Apply to intact skin; avoid contact with May require dose adjustment. Use caution.
eyes. • Do not wear when bathing/
showering. • Wash hands after SIDE EFFECTS
handling. Frequent (9%–4%): PO: Headache, abdomi-
INDICATIONS/ROUTES/DOSAGE nal cramps, constipation, diarrhea, nausea,
dyspepsia. Ophthalmic: Burning, stinging
Osteoarthritis on instillation, ocular discomfort. Occa-
PO: (Immediate-Release): ADULTS, sional (3%–1%): PO: Flatulence, dizziness,
ELDERLY: 50 mg 2–3 times/day. epigastric pain. Ophthalmic: Ocular
PO: (Extended-Release): ADULTS, itching, tearing. Rare (less than 1%):
ELDERLY:100 mg/day as a single dose. PO: Rash, peripheral edema, fluid retention,
(Zorvolex): 35 mg 3 times/day. visual disturbances, vomiting, drowsiness.
PO: (Delayed-Release): ADULTS,
ELDERLY: 50 mg 2–3 times/day or 75 mg ADVERSE EFFECTS/TOXIC
twice daily. REACTIONS
Topical gel: ADULTS, ELDERLY: Apply 4
times/day. Overdose may result in acute renal
failure. In pts treated chronically, pep-
Rheumatoid Arthritis (RA) tic ulcer, GI bleeding, gastritis, severe
PO: (Immediate-Release): ADULTS, hepatic reaction (jaundice), nephrotox-
ELDERLY: 50 mg 3–4 times/day. icity (hematuria, dysuria, proteinuria),

Canadian trade name Non-Crushable Drug High Alert drug


336 digoxin
severe hypersensitivity reaction (bron- USES
chospasm, angioedema) occur rarely.
Treatment of mild to moderate HF.
Control ventricular response rate in
NURSING CONSIDERATIONS pts with chronic atrial fibrillation. OFF-
LABEL: Fetal tachycardia with or without
D
BASELINE ASSESSMENT hydrops; decrease ventricular rate in
Obtain baseline B/P. Anti-inflamma- supraventricular tachyarrhythmias.
tory: Assess onset, type, location, dura-
tion of pain, inflammation. Inspect ap- PRECAUTIONS
pearance of affected joints for immobility, Contraindications: Hypersensitivity to
deformities, skin condition. digoxin. Ventricular fibrillation. Cau-
tions: Renal impairment, sinus nodal
INTERVENTION/EVALUATION disease, acute MI (within 6 mos), sec-
Monitor CBC, renal function, LFT, urine ond- or third-degree heart block (unless
output, occult blood test, B/P. Monitor for functioning pacemaker), concurrent
headache, dyspepsia. Monitor daily pat- use of strong inducers or inhibitors of
tern of bowel activity, stool consistency. P-­glycoprotein (e.g., cyclosporine),
Assess for therapeutic response: relief of hyperthyroidism, hypothyroidism, hypo-
pain, stiffness, swelling; increased joint kalemia, hypocalcemia.
mobility; reduced joint tenderness; im-
proved grip strength. ACTION
HF: Inhibits sodium/potassium ATPase
PATIENT/FAMILY TEACHING
pump in myocardial cells. Promotes
• Swallow tablets whole; do not chew, calcium influx. Supraventricular
crush, dissolve, or divide. • Avoid aspi- arrhythmias: Suppresses AV node
rin, alcohol during therapy (increases conduction. Therapeutic Effect: HF:
risk of GI bleeding). • If GI upset oc- Increases contractility. Supraventricu-
curs, take with food, milk. • Report lar arrhythmias: Increases effective
skin rash, itching, weight gain, changes refractory period/decreases conduc-
in vision, black stools, bleeding, jaun- tion velocity, decreases ventricular heart
dice, upper quadrant pain, persistent rate of fast atrial arrhythmias.
headache. • Ophthalmic: Do not use
hydrogel soft contact lenses. • Topi- PHARMACOKINETICS
cal: Avoid exposure to sunlight, sun- Route Onset Peak Duration
lamps. • Report rash. PO 0.5–2 hrs 2–8 hrs 3–4 days
IV 5–30 min 1–4 hrs 3–4 days

Readily absorbed from GI tract. Widely


digoxin distributed. Protein binding: 30%. Par-
tially metabolized in liver. Primarily
di-jox-in excreted in urine. Minimally removed
(Digitek, Digox, Lanoxin) by hemodialysis. Half-life: 36–48 hrs
Do not confuse digoxin with (increased in renal impairment, elderly).
Desoxyn or doxepin, or Lanoxin
with Lasix, Levoxyl, Levsinex, LIFESPAN CONSIDERATIONS
Lonox, or Mefoxin. Pregnancy/Lactation: Crosses pla­
centa. Distributed in breast milk.
uCLASSIFICATION Children: Premature infants more sus-
PHARMACOTHERAPEUTIC: Cardiac ceptible to toxicity. Elderly: Age-related
glycoside. CLINICAL: Antiarrhythmic. hepatic/renal impairment may require
dosage adjustment. Increased risk of loss
underlined – top prescribed drug
digoxin 337
of appetite. Avoid use as first-line therapy IV COMPATIBILITIES
for atrial fibrillation or HF. DilTIAZem (Cardizem), furosemide
(Lasix), heparin, insulin regular, lidocaine,
INTERACTIONS
midazolam (Versed), milrinone (Prima-
DRUG: Amiodarone may increase cor), morphine, potassium chloride.
concentration/toxicity. Beta blockers D
(e.g., metoprolol), calcium channel INDICATIONS/ROUTES/DOSAGE
blockers (e.g., dilTIAZem) may have Note: Loading dose not recommended
additive effect on slowing AV nodal con- in HF.
duction. Potassium-depleting diuret-
ics (e.g., furosemide) may increase Loading Dose
toxicity due to hypokalemia. Ketocon- PO: ADULTS, ELDERLY: 0.75–1.5 mg.
azole, vemurafenib may increase CHILDREN 10 YRS AND OLDER: 10–15
concentration/effect. Sucralfate may mcg/kg. CHILDREN 5–9 YRS: 20–35 mcg/
decrease absorption/concentration. kg. CHILDREN 2–4 YRS: 30–40 mcg/kg.
HERBAL: Licorice may increase adverse CHILDREN 1–23 MOS: 35–60 mcg/kg.
effects. FOOD: Meals with increased NEONATES, FULL-TERM: 25–35 mcg/kg.
fiber (bran) or high in pectin may NEONATES, PREMATURE: 20–30 mcg/kg.
decrease absorption. LAB VALUES: None IV: ADULTS, ELDERLY: 0.5–1 mg. CHIL-
known. DREN 10 YRS AND OLDER: 8–12 mcg/kg.
CHILDREN 5–9 YRS: 15–30 mcg/kg. CHIL-
AVAILABILITY (Rx) DREN 2–4 YRS: 25–35 mcg/kg. CHILDREN
Oral Solution: (Lanoxin): 50 mcg/mL. 1–23 MOS: 30–50 mcg/kg. NEONATES,
Injection Solution: (Lanoxin): 100 mcg/ FULL-TERM: 20–30 mcg/kg. NEONATES,
mL, 250 mcg/mL. Tablets: (Lanoxin): 62.5 PREMATURE: 15–25 mcg/kg.
mcg, 125 mcg, 187.5 mcg, 250 mcg.
Maintenance Dosage
ADMINISTRATION/HANDLING PO IV/IM
b ALERT c IM rarely used (produces Preterm 5–7.5 mcg/kg 4–6 mcg/kg
severe local irritation, erratic absorp- infant
tion). If no other route possible, give Full-term 8–10 mcg/kg 5–8 mcg/kg
deep into muscle followed by massage. infant
1 mo–2 10–15 mcg/kg 9–15 mcg/kg
Give no more than 2 mL at any one site.
yrs
IV 2–5 yrs 8–10 mcg/kg 6–9 mcg/kg
5–10 yrs 5–10 mcg/kg 4–8 mcg/kg
• May give undiluted or dilute with at
least a 4-fold volume of Sterile Water for Note: Avoid doses greater than 0.125
Injection or D5W (less may cause pre- mg/day in elderly due to decreased renal
cipitate). • Use immediately. • Give clearance.
IV slowly over at least 5 min.
HF
PO PO: ADULTS, ELDERLY: 0.125–0.25 mg
• May give without regard to once daily.
food. • Tablets may be crushed.
Atrial Fibrillation
IV INCOMPATIBILITIES ADULTS, ELDERLY: Digitalizing dose
Amphotericin B complex (Abelcet, AmBi- (IV): Initially, 0.25–0.5 mg over several
some, Amphotec), fluconazole (Diflu- minutes. May repeat doses of 0.25 mg q6
can), foscarnet (Foscavir), propofol hrs up to a maximum of 1.5 mg over 24 hrs.
(Diprivan). Maintenance dose (PO): 0.125–0.25
mg once daily.

Canadian trade name Non-Crushable Drug High Alert drug


338 dihydroergotamine
Dosage in Renal Impairment for GI disturbances, neurologic abnor-
Dosage adjustment is based on creatinine malities (signs of toxicity) q2–4h during
clearance. Loading dose: Decrease by loading dose (daily during maintenance).
50% in end-stage renal disease. Monitor serum potassium, magnesium,
calcium, renal function. Therapeutic
D Maintenance Dose serum level: 0.8–2 ng/mL; toxic serum
eGFR Dosage level: greater than 2 ng/mL.
10–50 mL/min 25%–75% of usual
dose or q36h (0.0625 PATIENT/FAMILY TEACHING
mg q24–36hrs) • Follow-up visits, blood tests are an im-
Less than 10%–25% of usual portant part of therapy. • Follow guide-
10 mL/min dose or q48h (0.0625 lines to take apical pulse and report pulse
(HD, PD, CRRT) mg q48h)
of 60 or less/min (or as indicated by physi-
cian). • Wear/carry identification of di-
Dosage in Hepatic Impairment goxin therapy and inform dentist, other
No dose adjustment. physician of taking digoxin. • Do not in-
crease or skip doses. • Do not take OTC
SIDE EFFECTS medications without consulting physi-
Dizziness, headache, diarrhea, rash, cian. • Report decreased appetite, nau-
visual disturbances. sea/vomiting, diarrhea, visual changes.
ADVERSE EFFECTS/TOXIC
REACTIONS dihydroergotamine
The most common early manifestations
of digoxin toxicity are GI disturbances dye-hye-droe-er-got-a-meen
(anorexia, nausea, vomiting), neuro- (D.H.E. 45, Migranal)
logic abnormalities (fatigue, headache, j BLACK BOX ALERT jConcur-
depression, weakness, drowsiness, rent use with CYP3A4 inhibitors
confusion, nightmares). Facial pain, (macrolide antibiotics, azole
personality change, ocular disturbances antifungals, protease inhibitors)
(photophobia, light flashes, halos around increases risk of vasospasm,
producing ischemia of brain and
bright objects, yellow or green color per- peripheral extremities.
ception) may occur. Sinus bradycardia,
AV block, ventricular arrhythmias noted. FIXED-COMBINATION(S)
Antidote: Digoxin immune FAB (see Cafergot, Wigraine: ergotamine/
Appendix J for dosage). caffeine (stimulant): 1 mg/100 mg,
2 mg/100 mg.
NURSING CONSIDERATIONS Do not confuse Cafergot with Ca-
BASELINE ASSESSMENT rafate.
Assess apical pulse. If pulse is 60 or uCLASSIFICATION
less/min (70 or less/min for children),
withhold drug, contact physician. Blood PHARMACOTHERAPEUTIC: Ergot-
samples are best taken 6–8 hrs after dose amine derivative. CLINICAL: Antimi-
or just before next dose. graine agent.
INTERVENTION/EVALUATION
Monitor pulse for bradycardia, ECG for
USES
arrhythmias for 1–2 hrs after adminis- Treatment of migraine headache with or
tration (excessive slowing of pulse may without aura. Injection also used to treat
be first clinical sign of toxicity). Assess cluster headache.

underlined – top prescribed drug


dihydroergotamine 339

PRECAUTIONS disease increases risk of peripheral


Contraindications: Hypersensitivity vasoconstriction. Age-related renal
to dihydroergotamine. Uncontrolled impairment may require dosage
hypertension, ischemic heart disease, adjustment.
coronary artery vasospasm (including
INTERACTIONS D
Prinzmetal’s angina), angina pectoris,
history of MI following vascular surgery, DRUG: Ergot derivatives (e.g.,
concurrent use of peripheral and central ergotamine), 5-HT1B agonists (e.g.,
vasoconstrictors, hemiplegic or basilar SUMAtriptan), systemic vasocon-
migraine, peripheral vascular disease, strictors (e.g., DOBUTamine, phen-
sepsis, severe renal/hepatic impairment, ylephrine) may increase vasopressor
use of MAOIs within 14 days, use of effect. Strong CYP3A4 inhibitors
SUMAtriptan, ZOLMitriptan, other sero- (e.g., clarithromycin, ketoconazole,
tonin agonists, or ergot-like agents within ritonavir) may increase concentration/
24 hrs, potent CYP3A4 inhibitors (e.g., effect. Enzalutamide may decrease
azole antifungals, macrolide antibiotics, concentration/effect. May decrease
protease inhibitors), pregnancy, breast- therapeutic effect of nitroglycerin.
feeding. Cautions: Elderly. HERBAL: None significant. FOOD: Cof-
fee, cola, tea may increase absorption.
ACTION Grapefruit products may increase con-
Binds to serotonin, norepinephrine, and centration, toxicity. LAB VALUES: None
dopamine receptors. Efficacy in migraine significant.
is attributed to activation of serotonin
receptors located on intracranial blood AVAILABILITY (Rx)
vessels, causing vasoconstriction and/or Dihydroergotamine Injection, Solution:
sensory nerve endings of the trigeminal 1 mg/mL. Intranasal Spray, Solution:
system, resulting in inhibiting pro-inflam- (Migranal): 4 mg/mL (0.5 mg/spray).
matory neuropeptide release. Thera-
peutic Effect: Suppresses vascular INDICATIONS/ROUTES/DOSAGE
headaches, migraine headaches. Migraine Headache
IM/SQ: ADULTS, ELDERLY: 1 mg at onset
PHARMACOKINETICS of headache; repeat hourly up to a maxi-
Slowly, incompletely absorbed from GI mum of 3 mg/day; 6 mg/wk.
tract; rapidly and extensively absorbed IV: ADULTS, ELDERLY: (Give slowly over
after rectal administration. Protein bind- 2–3 min) 1 mg at onset of headache;
ing: greater than 90%. Eliminated in feces repeat hourly up to a maximum of 2 mg/
by the biliary system. Half-life: 21 hrs. day; 6 mg/wk.
Intranasal: ADULTS, ELDERLY: 1 spray
LIFESPAN CONSIDERATIONS (0.5 mg) into each nostril; repeat in 15
Pregnancy/Lactation: Contraindi- min up to a total of 4 sprays (2 mg). Do
cated in pregnancy (produces uterine not exceed 6 sprays (3 mg) in 24-hr
stimulant action, resulting in possible period or 8 sprays (4 mg) in a wk.
fetal death or retarded fetal growth);
increases vasoconstriction of placental Dosage in Renal/Hepatic Impairment
vascular bed. Drug distributed in breast Contraindicated in severe impairment.
milk. May produce diarrhea, vomiting SIDE EFFECTS
in neonate. May prohibit lactation.
Occasional (5%–2%): Cough, dizziness.
Children: No precautions in pts 6 yrs
Rare (less than 2%): Myalgia, fatigue,
and older, but use only when unrespon-
sive to other medication. Elderly: Age- diarrhea, upper respiratory tract infec-
related occlusive peripheral vascular tion, dyspepsia.

Canadian trade name Non-Crushable Drug High Alert drug


340 dilTIAZem

ADVERSE EFFECTS/TOXIC Do not confuse Cardizem


REACTIONS with Cardene or Cardene SR,
Prolonged administration, excessive Cartia XT with Procardia XL,
dosage may produce ergotamine poi- dilTIAZem with Calan, diaz-
soning, manifested as nausea, vomiting, ePAM, or Dilantin, or Tiazac
D paresthesia of extremities, muscle pain/ with Ziac.
weakness, precordial pain, significant
FIXED-COMBINATION(S)
changes in pulse rate and blood pres-
sure. Vasoconstriction of peripheral Teczem: dilTIAZem/enalapril (ACE in-
arteries/arterioles may result in localized hibitor): 180 mg/5 mg.
edema, pruritus; feet, hands will become uCLASSIFICATION
cold, pale. Muscle pain will occur when
walking and later, even at rest. Other rare PHARMACOTHERAPEUTIC: Calcium
effects include confusion, depression, channel blocker. Non-dihydropyri-
drowsiness, seizures, gangrene. dine. CLINICAL: Antianginal, antihy-
pertensive, class IV antiarrhythmic.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT USES
Question for history of peripheral vascu- PO: Treatment of angina due to coro-
lar disease, renal/hepatic impairment, nary artery spasm (Prinzmetal’s vari-
possibility of pregnancy. Question onset, ant angina), chronic stable angina
location, duration of migraine, possible (effort-associated angina). Treatment of
precipitating symptoms. Obtain full med- hypertension. Parenteral: Temporary
ication history and screen for interac- control of rapid ventricular rate in atrial
tions. Obtain B/P. fibrillation/flutter. Rapid conversion of
INTERVENTION/EVALUATION paroxysmal supraventricular tachycardia
(PSVT) to normal sinus rhythm.
Monitor closely for evidence of ergotamine
overdosage as result of prolonged admin- PRECAUTIONS
istration or excessive dosage. Monitor B/P.
Contraindications: PO: Hypersensitiv-
PATIENT/FAMILY TEACHING ity to dilTIAZem, acute MI, pulmonary
• Initiate therapy at first sign of migraine congestion, second- or third-degree AV
headache. • Report if there is need to block (except in presence of pacemaker),
progressively increase dose to relieve vas- severe hypotension (less than 90 mm Hg,
cular headaches or if palpitations, nausea, systolic), sick sinus syndrome (except in
vomiting, paresthesia, pain or weakness of presence of pacemaker). IV: Hypersen-
extremities, chest pain. Avoid grapefruit sitivity to dilTIAZem. Sick sinus syndrome
products. • Female pts should avoid or second- or third-degree block (except
pregnancy; if suspected, immediately re- with functioning pacemaker), cardiogenic
port. • Do not use triptans for 24 hrs shock, administration of IV beta blocker
after last dose of dihydroergotamine. within several hours, atrial fibrillation/flut-
ter associated with accessory bypass tract,
severe hypotension, ventricular tachycar-
dia. Cautions: Renal/hepatic impairment,
dilTIAZem HF, concurrent use with beta blocker,
hypertrophic obstructive cardiomyopathy.
dil-tye-a-zem
(Apo-Diltiaz , Cardizem, Cardizem ACTION
CD, Cardizem LA, Cartia XT, Dilt-XR, Inhibits calcium movement across
Matzim LA, Taztia XT, Tiazac) cardiac, vascular smooth-muscle cell
underlined – top prescribed drug
dilTIAZem 341
membranes (causes dilation of coronary Immediate-Release: 30 mg, 60 mg, 90
arteries, peripheral arteries, arterioles) mg, 120 mg.
during depolarization. Therapeu- Capsules, Extended-Release, 24
tic Effect: Relaxes coronary vascular Hour: 120 mg, 180 mg, 240 mg, 300 mg,
smooth muscle, and coronary vasodila- 360 mg, 420 mg. Capsules, Extended-
tion increases myocardial oxygen deliv- Release, 12 Hour: 60 mg, 90 mg, 120 mg.
D
ery in pts with vasospastic angina. Tablets, Extended-Release, 24 Hour:
PHARMACOKINETICS 120 mg, 180 mg, 240 mg, 300 mg, 360
mg, 420 mg.
Route Onset Peak Duration
PO 0.5–1 hr N/A N/A ADMINISTRATION/HANDLING
PO (extended- 2–3 hrs N/A N/A
release) IV
IV 3 min N/A N/A Reconstitution • Add 125 mg to 100
Well absorbed from GI tract. Protein mL D5W, 0.9% NaCl to provide concen-
binding: 70%–80%. Primarily excreted tration of 1 mg/mL.
in urine. Not removed by hemodialysis. Rate of administration • Infuse per
Half-life: 3–8 hrs. dilution/rate chart provided by
manufacturer.
LIFESPAN CONSIDERATIONS Storage • Refrigerate vials. • After
Pregnancy/Lactation: Distributed in dilution, stable for 24 hrs.
breast milk. Children: No age-related PO
precautions noted. Elderly: Age-related • Give immediate-release tablets before
renal impairment may require dosage meals and at bedtime. • Tablets may be
adjustment. crushed. • Do not break, crush, dis-
INTERACTIONS solve, or divide sustained-release capsules
or extended-release capsules or tab-
DRUG: Beta blockers (e.g., atenolol, lets. • Taztia XT capsules may be opened
carvedilol, metoprolol) may increase and mixed with applesauce; follow with
effects; risk of bradycardia. Statins (e.g., glass of water. • Cardizem CD, Cardizem
atorvastatin, simvastatin), strong LA, Cartia XT, Matzim LA may be given
CYP3A4 inhibitors (e.g., clarithro- without regard to food. • Dilacor XR,
mycin, ketoconazole, ritonavir) may Dilt-XR to be given on empty stomach.
increase concentration/effect. Strong
CYP3A4 inducers (e.g., carBAMaze- IV INCOMPATIBILITIES
pine, phenytoin, rifAMPin) may decrease AcetaZOLAMIDE (Diamox), acyclovir
concentration/effect. May increase concen- (Zovirax), ampicillin, ampicillin/sul-
tration/effects of bosutinib, budesonide. bactam (Unasyn), diazePAM (Valium),
HERBAL: Ephedra, St. John’s wort,
furosemide (Lasix), heparin, insulin,
yohimbe may decrease concentration/ nafcillin, phenytoin (Dilantin), rifAMPin
effect. Herbals with hypotensive proper- (Rifadin), sodium bicarbonate.
ties (e.g., garlic, ginger, gingko biloba)
may increase effect. St. John’s wort may IV COMPATIBILITIES
decrease concentration. FOOD: Grapefruit Albumin, aztreonam (Azactam), bu­ m­
products may increase concentration/effect. e­
tanide (Bumex), ceFAZolin (Ancef),
LAB VALUES: ECG: May increase PR interval.
cefotaxime (Claforan), cefTAZidime
AVAILABILITY (Rx) (Fortaz), cefTRIAXone (Rocephin), cefu-
roxime (Zinacef), ciprofloxacin (Cipro),
25 mg/5 mL, 50
Injection, Solution:
clindamycin (Cleocin), dexmedetomi-
mg/10 mL, 125 mg/25 mL. Tablets, dine (Precedex), digoxin (Lanoxin),

Canadian trade name Non-Crushable Drug High Alert drug


342 dilTIAZem
DOBUTamine (Dobutrex), DOPamine PO: (Extended-Release Tablet [once-
(Intropin), gentamicin, HYDROmor- daily dosing]): (Cardizem LA, Matzim
phone (Dilaudid), lidocaine, LORazepam LA): ADULTS, ELDERLY: Initially, 180–240
(Ativan), metoclopramide (Reglan), mg/day. May increase at 14-day inter-
metroNIDAZOLE (Flagyl), midazolam vals. Range: 120–360 mg/day. Maxi-
D (Versed), morphine, multivitamins, ni- mum: 540 mg/day.
troglycerin, norepinephrine (Levophed),
potassium chloride, potassium phos- Temporary Control of Rapid Ventricular
phate, tobramycin (Nebcin), vancomycin Rate in Atrial Fibrillation/Flutter; Rapid
(Vancocin). Conversion of Paroxysmal Supraventricular
Tachycardia to Normal Sinus Rhythm
INDICATIONS/ROUTES/DOSAGE IV bolus: ADULTS, ELDERLY: Initially,
Angina 0.25 mg/kg (average dose: 20 mg) actual
PO: (Immediate-Release): ADULTS, body weight over 2 min. May repeat in 15
ELDERLY: Initially, 30 mg 4 times/day. min at dose of 0.35 mg/kg (average dose:
Range: 120–320 mg/day. 25 mg) actual body weight. Subsequent
PO: (Extended-Release) (Cardizem doses individualized.
CD, Cartia XT, DILT-XR): ADULTS, IV infusion: ADULTS, ELDERLY: After ini-
ELDERLY: Initially, 120–180 mg once tial bolus injection, may begin infusion at
daily. May increase at 7- to 14-day 5–10 mg/hr; may increase by 5 mg/hr up
intervals. Range: 120–320 mg. Maxi- to a maximum of 15 mg/hr. Continuous
mum: 480 mg/day (540 mg for Cardi- infusion longer than 24 hrs or infusion
zem CD, Cartia XT). rate greater than 15 mg/hr are not rec-
(Extended-Release) (Tiazac, Taztia ommended. Attempt conversion to PO
XT): ADULTS, ELDERLY: Initially, 120–180 therapy as soon as possible.
mg once daily. May increase at 7- to Dosage in Renal/Hepatic Impairment
14-day intervals. Range: 120–320 mg/ Use with caution.
day. Maximum: 540 mg/day.
(Extended-Release) (Cardizem LA, SIDE EFFECTS
Matzim LA): Initially, 180 mg/day.
Frequent (10%–5%): Peripheral edema,
May increase at 7- to 14-day intervals. dizziness, light-headedness, headache,
Range: 120–320 mg. Maximum: 360 bradycardia, asthenia. Occasional
mg daily. (5%–2%): Nausea, constipation, flush-
Hypertension ing, ECG changes. Rare (less than
PO: (Extended-Release Capsule 2%): Rash, micturition disorder (poly-
[once-­daily dosing]): (Cardizem CD, uria, nocturia, dysuria, frequency of
Cartia XT): Initially, 180–240 mg/day. urination), abdominal discomfort,
May increase after 14 days. Usual dose: drowsiness.
240–360 mg/day. Maximum: 480 mg/ ADVERSE EFFECTS/TOXIC
day. (Dilt-XR): Initially, 180–240 mg/day. REACTIONS
May increase after 14 days. Usual dose:
240–360 mg/day. Maximum: 540 mg/ Abrupt withdrawal may increase fre-
day. (Tiazac, Taztia XT): Initially, 120– quency, duration of angina, HF; sec-
240 mg/day. Usual dose: 120–360 mg/ ond- or third-degree AV block occurs
day. Maximum: 540 mg/day. rarely. Overdose produces nausea,
PO: (Extended-Release Capsule drowsiness, confusion, slurred speech,
[twice-daily dosing]): ADULTS, profound bradycardia. Antidote: Glu-
ELDERLY: Initially, 60–120 mg twice cagon, insulin drip with continuous
daily. May increase at 14-day intervals. calcium infusion (see Appendix J for
Maintenance: 120–180 mg twice daily. dosage).

underlined – top prescribed drug


dimethyl fumarate 343

NURSING CONSIDERATIONS transaminases, lymphopenia (may


decrease lymphocyte count).
BASELINE ASSESSMENT
Record onset, type (sharp, dull, squeez- ACTION
ing), radiation, location, intensity, dura- Exact mechanism of action unknown.
tion of anginal pain, precipitating fac- May include anti-inflammatory action and D
tors (exertion, emotional stress). Assess cytoprotective properties. Therapeutic
baseline renal/hepatic function tests. As- Effect: Modifies disease progression.
sess B/P, apical pulse immediately before PHARMACOKINETICS
drug is administered. Obtain baseline
ECG in pts with history of arrhythmia. Undergoes rapid hydrolysis into active
metabolite, monomethyl fumarate. Peak
INTERVENTION/EVALUATION concentration: 2–212 hrs. Protein bind-
Assist with ambulation if dizziness oc- ing: 27%–45%. Extensively metabolized by
curs. Assess for peripheral edema. Moni- esterases. Primarily eliminated as exhaled
tor pulse rate for bradycardia. Assess B/P, carbon dioxide (60%). Half-life: 1 hr.
renal function, LFT, ECG with IV therapy.
Question for asthenia, headache. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown
PATIENT/FAMILY TEACHING
if dis­
tributed in breast milk. Chil-
• Do not abruptly discontinue medica- dren: Safety and efficacy not estab-
tion. • Compliance with therapy regimen lished. Elderly: No age-related
is essential to control anginal pain. • To precautions noted.
avoid postural dizziness, go from lying to
standing slowly. • Avoid tasks that re- INTERACTIONS
quire alertness, motor skills until response DRUG: May decrease therapeutic effects;
to drug is established. • Report palpita- increase adverse effects of vaccines (live).
tions, shortness of breath, pronounced HERBAL: None known. FOOD: None sig-
dizziness, nausea, constipation. • Avoid nificant. LAB VALUES: May decrease lym-
alcohol (may increase risk of hypotension phocytes. May increase serum ALT, AST;
or vasodilation). eosinophils; urine albumin.

AVAILABILITY (Rx)
dimethyl fumarate Capsules, Delayed-Release: 120 mg, 240
mg.
dye-meth-il-fue-ma-rate
(Tecfidera) ADMINISTRATION/HANDLING
PO
uCLASSIFICATION
• Give capsule whole; do not break,
PHARMACOTHERAPEUTIC: Fumaric crush, dissolve, or divide. • May give
acid agent. CLINICAL: Multiple scle- without regard to food. May give with
rosis agent. Immunomodulator. food to decrease flushing reaction and GI
effects. • Protect from light.
USES INDICATIONS/ROUTES/DOSAGE
Treatment of relapsing-remitting multiple Relapsing-Remitting Multiple Sclerosis
sclerosis. PO: ADULTS/ELDERLY: Initially, 120 mg
PRECAUTIONS twice daily for 7 days. Then, increase to
Hypersensitivity to
Contraindications:
240 mg twice daily.
dimethyl fumarate. Cautions: Hepatic Dosage in Renal/Hepatic Impairment
impairment (may increase hepatic No dose adjustment.
Canadian trade name Non-Crushable Drug High Alert drug
344 dinutuximab

SIDE EFFECTS including antihistamines, prior to


each infusion. Treatment causes
Frequent (40%): Flushing. Occasional severe neuropathic pain. Administer
(18%–5%): Abdominal pain, diarrhea, IV opioids prior to each infusion and
nausea, vomiting, dyspepsia, pruritus, for 2 hrs following completion of
rash, erythema. infusion. Severe peripheral sensory
D neuropathy occurred in pts with
ADVERSE EFFECTS/TOXIC neuroblastoma. Severe motor neu-
ropathy was observed. Discontinue
REACTIONS therapy if severe unresponsive
Lymphopenia may increase risk for infec- pain, severe sensory neuropathy, or
tion. Severe flushing may lead to non- moderate to severe peripheral motor
compliance of therapy. neuropathy occurs.
Do not confuse dinutuximab
NURSING CONSIDERATIONS with brentuximab, cetuximab,
riTUXimab, or siltuximab.
BASELINE ASSESSMENT
Obtain baseline CBC, CMP, urine preg- uCLASSIFICATION
nancy if applicable. Question any plans PHARMACOTHERAPEUTIC: GD2-
of breastfeeding. Assess hydration status binding monoclonal antibody. CLINI-
(urine output, skin turgor). Question his- CAL: Antineoplastic.
tory of hepatic impairment, lymphopenia.
INTERVENTION/EVALUATION USES
Monitor CBC, LFT. Encourage PO intake. Used in combination with granulocyte-
Offer antiemetics for nausea, vomiting. macrophage colony-stimulating factor
Question any episodes of noncompliance (GM-CSF), interleukin-2 (IL-2), and 13-cis-
due to flushing, GI symptoms. Monitor retinoic acid for the treatment of pediatric
for infectious process (fever, malaise, pts with high-risk neuroblastoma who
chills, body aches, cough). achieve at least a partial response to prior
fine-line multiagent, multimodality therapy.
PATIENT/FAMILY TEACHING
• Pts will most likely experience abdomi- PRECAUTIONS
nal pain, diarrhea, nausea, and flushing. Contraindications: History of anaphy-
Side effects may decrease over time. • Take laxis to dinutuximab. Cautions: Active
with meals to decrease flushing reac- infection; baseline cytopenias; diabe-
tion. • Swallow capsule whole; do not tes, dehydration, electrolyte imbalance,
chew, crush, dissolve, or divide. • Two hepatic/renal impairment, peripheral or
dosage strengths will be provided for start- generalized edema; intolerance of opi-
ing dose and maintenance dose. • Report oids, antipyretics, antihistamines; history
any yellowing of skin or eyes, upper ab- of arrhythmias, hypotension, neuropathy,
dominal pain, bruising, dark-colored urine, optic disorders.
fever, body aches, cough, dehydration.
ACTION
Binds to glycolipid GD2 expressed
on neuroblastoma cells and on nor-
dinutuximab mal cells of neuroectodermal origin,
including CNS and peripheral nerves.
din-ue-tux-i-mab Induces cell lysis of GD2-expressing
(Unituxin) cells through antibody-dependent cell-
j BLACK BOX ALERT jLife-threat- mediated cytotoxicity and complement-
ening infusion-related reactions dependent cytotoxicity. Therapeutic
have occurred. Administer required Effect: Inhibits tumor cell growth and
prehydration and premedication, metastasis.
underlined – top prescribed drug
dinutuximab 345

PHARMACOKINETICS additional doses of morphine sulfate


Widely distributed. Metabolism not speci- 25–50 mcg/kg IV once every 2 hrs as
fied. Protein binding: not specified. Elim- needed for pain, followed by an increase
ination not specified. Half-life: 10 days. in morphine infusion rate, if clinically
stable. • Consider use of fentaNYL or
LIFESPAN CONSIDERATIONS HYDROmorphone if morphine sulfate D
Pregnancy/Lactation: Avoid preg- not tolerated. • If pain is inadequately
nancy; may cause fetal harm, esp. in third controlled with opioids, consider use of
trimester. Unknown if distributed in breast gabapentin or lidocaine in addition to IV
milk. However, human immunoglobulin morphine.
G is present in human breast milk. Must Antihistamines and antipyretics
either discontinue drug or discontinue • Administer an antihistamine such as
breastfeeding. Females of reproductive diphenhydrAMINE 0.5–1 mg/kg (maxi-
potential must use effective contraception mum dose 50 mg) IV over 10–15 min,
during treatment and for at least 2 mos fol- starting 20 min prior to initiation and
lowing discontinuation. Children: No age- as tolerated every 4–6 hrs during infu-
related precautions noted. Elderly: Safety sion. • Administer acetaminophen
and efficacy not established. 10–15 mg/kg (maximum dose 650
mg) 20 minutes prior to each infusion
INTERACTIONS and every 4–6 hrs as needed for fever/
DRUG: May decrease therapeutic pain. • May administer ibuprofen 5–10
effect of BCG (intravesical), vac- mg/kg every 6 hrs as needed for persis-
cines (live). May increase adverse tent fever/pain.
effects of belimumab, natalizumab, Preparation of infusion • Visually
vaccines (live). HERBAL: Echina- inspect for particulate matter or discol-
cea may decrease therapeutic effect. oration. Do not use if solution is cloudy
FOOD: None known. LAB VALUES: May or contains particulate matter. • With-
decrease Hgb, Hct, lymphocytes, neu- draw required volume from vial and
trophils, platelets, RBCs; serum albu- inject into 100 mL 0.9% NaCl. • Mix
min, calcium, magnesium, phosphate, by gentle inversion. Do not shake or agi-
potassium, sodium. May increase serum tate. • Discard unused portions of vial.
ALT, AST, bilirubin, creatinine, glucose; Rate of administration • Initiate
urine protein. infusion rate at 0.875 mg/m2/hr for 30
min via dedicated IV line. May gradually
AVAILABILITY (Rx) increase rate to maximum rate of 1.75/
Injection Solution: 17.5 mg/5 mL (3.5 m2/hr as tolerated. • Do not infuse as
mg/mL). IV push or bolus.
Storage • Refrigerate vials. • Pro-
ADMINISTRATION/HANDLING tect from light by storing in outer car-
ton. • May refrigerate diluted solution
IV
up to 4 hrs. • Discard diluted solution
Pretreatment Guidelines 24 hrs after preparation.
Hydration • Administer bolus of 0.9%
NaCl 10 mL/kg IV over 1 hr prior to IV INCOMPATIBILITIES
initiation. Do not mix with other medications.
Analgesics • Administer morphine
sulfate 50 mcg/kg IV immediately prior INDICATIONS/ROUTES/DOSAGE
to initiation and then continue as mor- Neuroblastoma
phine sulfate drip at rate of 20–50 mcg/ IV: PEDIATRIC:17.5 mg/m2/day over
kg/hr during and for 2 hrs following 10–20 hrs for 4 consecutive days for
completion of infusion. • Administer maximum of 5 cycles (Tables 1 and 2).

Canadian trade name Non-Crushable Drug High Alert drug


346 dinutuximab
TABLE 1 SCHEDULE OF DINUTUXIMAB ADMINISTRATION FOR CYCLES 1, 3, AND 5
Cycle Day 1 through 3 4 5 6 7 8 through 24*
dinutuximab X X X X
*Cycles 2 and 4 are 32 days in duration.
D TABLE 2 SCHEDULE OF DINUTUXIMAB ADMINISTRATION FOR CYCLES 2 AND 4
Cycle Day 1 through 7 8 9 10 11 12 through 32*
dinutuximab X X X X
*Cycles 2 and 4 are 32 days in duration.

Dose Modification previous rate. If blood pressure remains


Infusion-Related Reactions stable for at least 2 hrs, increase infusion
Mild to moderate adverse reactions rate as tolerated up to maximum rate of
(transient rash, fever, rigors, or local- 1.75 mg/m2/hr.
ized urticaria that respond promptly
to symptomatic treatment): Decrease Infection
infusion rate to 50% of the previous rate. Severe systemic infection or sepsis:
Once resolved, gradually increase infusion Discontinue treatment until infection
rate up to a maximum rate of 1.75 mg/m2/ resolves, then continue with subsequent
hr. Prolonged or severe adverse reac- cycles of treatment.
tions (mild bronchospasm without
Neurologic Disorders of the Eye
other symptoms, angioedema that
Dilated pupil with sluggish reflex;
does not affect the airway): Immedi-
other visual disturbances: Interrupt
ately interrupt infusion. If symptoms resolve infusion. Once resolved, resume infusion
rapidly, restart infusion at 50% of the pre- rate at 50% of previous rate. First recur-
vious rate. First recurrence of severe rence or if accompanied by visual
reaction: Discontinue treatment until the
impairment: Permanently discontinue.
following day. If symptoms resolve and
continued treatment is still warranted, pre- Adverse Reactions Requiring Permanent
medicate with hydrocortisone (per guide- Discontinuation (based on Common
lines) and administer dinutuximab infusion Terminology for Adverse Events [CTCAE])
at a rate of 0.875 mg/m2/hr in an intensive Grade 3 or 4 anaphylaxis, serum sick-
care unit. Second recurrence of severe ness; Grade 3 pain unresponsive to
reaction: Permanently discontinue. maximum supportive measures; Grade
Capillary Leak Syndrome
4 sensory neuropathy or Grade 3 sen-
Moderate to severe, non–life-threat-
sory neuropathy that interferes with daily
ening capillary leak syndrome:
activities for more than 2 wks; Grade 2
Interrupt infusion. Once resolved, resume peripheral motor neuropathy, subtotal or
infusion rate at 50% of previous rate. total vision loss; Grade 4 hyponatremia
Life-threatening capillary leak syn-
despite appropriate fluid management.
drome: Discontinue treatment for the Dosage in Renal/Hepatic Impairment
current cycle. Once resolved, administer Not specified; use caution.
at 50% of the previous rate for subsequent
cycles. First recurrence: Permanently SIDE EFFECTS
discontinue. Frequent (85%–24%): Pain (abdominal,
Hypotension back, bladder, bone, chest, neck, facial,
Hypotension requiring medical gingival, musculoskeletal, oropharyngeal,
intervention: Interrupt infusion. Once extremity), arthralgia, myalgia, neuralgia,
resolved, resume infusion rate at 50% of proctalgia, pyrexia, hypotension, vomiting,

underlined – top prescribed drug


dinutuximab 347
diarrhea, urticaria, hypoxia. Occasional NURSING CONSIDERATIONS
(19%–10%): Tachycardia, edema, hyper-
tension, peripheral neuropathy, weight BASELINE ASSESSMENT
gain, nausea. Obtain baseline CBC, BMP, LFT; serum
magnesium, ionized calcium, prealbu-
ADVERSE EFFECTS/TOXIC min, phosphate triglyceride level; capillary D
REACTIONS blood glucose, urinalysis, urine protein,
Anemia, neutropenia, lymphopenia, throm- urine pregnancy test, vital signs. Verify that
bocytopenia are expected results of therapy. pts have adequate hematologic/hepatic/
Severe bone marrow suppression occurred ophthalmic/respiratory/renal function and
in up to 39% of pts. Serious infusion-related proper hydration status prior to start of
reactions, such as bronchospasm, dyspnea, each infusion. Ensure proper resuscitative
facial and upper airway edema, hypoten- equipment/medications are readily avail-
sion, or stridor, may require urgent inter- able. Obtain baseline visual acuity, pupillary
ventions, including bronchodilator therapy, response, neurologic status. Question his-
blood pressure support, corticosteroids, tory of anaphylaxis; intolerance of opioids,
infusion interruption, infusion rate reduc- antipyretics, antihistamines. Screen for ac-
tion, or permanent treatment discontinua- tive infection. Offer emotional support.
tion. Severe infusion-related reactions were
reported in 26% of pts. Infusion-related INTERVENTION/EVALUATION
reactions usually occurred during or within Frequently monitor CBC, BMP, LFT, other
24 hrs of infusion completion. Other seri- serum electrolytes, vital signs. Monitor
ous adverse effects may include: severe I&O. Administer required prehydration
urticaria (13% of pts); anaphylaxis, cardiac and premedication with antihistamine,
arrest (1% or less of pts); pain despite pre- antipyretics, opioids prior to each infusion
treatment with analgesics including mor- and during infusion as indicated. Diligently
phine sulfate infusion (85% of pts); Grade monitor for infusion-related reactions as
3 pain (51% of pts); Grade 3 peripheral listed in Adverse Effects/Toxic Reactions
sensory/motor neuropathy (1% of pts); and institute medical support as needed.
Grade 3–5 capillary leak syndrome (23% Monitor for bleeding events of any kind.
of pts); Grade 3 hypotension (16% of pts); Consider administration of naloxone if
Grade 3 or 4 bacteremia requiring IV anti- narcotic overdose is suspected. Routinely
biotics or other urgent interventions (13% assess visual acuity, hydration status. Offer
of pts); sepsis (18% of pts); neurologic dis- emotional support. Initiate fall precautions.
orders of the eye, including blurred vision, PATIENT/FAMILY TEACHING
photophobia, mydriasis, fixed or unequal
pupils, optic nerve disorder, eyelid ptosis, • Serious infusion reactions, including
papilledema (2%–13% of pts); Grade 3 anaphylaxis, difficulty breathing, facial
or 4 electrolyte abnormalities, including swelling, itching, rash, and wheezing, may
hyponatremia, hypokalemia, hypocalce- occur during or within 24 hrs of each infu-
mia (37%–23% of pts); atypical hemolytic sion. • Immediately report any allergic
uremic syndrome resulting in anemia, reactions; bleeding of any kind; decreased
electrolyte imbalance, hypertension, renal urine output or dark urine; disorders of the
insufficiency. Bleeding events, including GI/ eye including blurry vision, double vision,
rectal/renal/respiratory/urinary tract/cathe- unequal pupil size, sensitivity to light, eyelid
ter site hemorrhage, disseminated intravas- drooping; fever; palpitations; seizures (re-
cular coagulation, epistaxis, hematemesis, lated to electrolyte imbalance); severe
hematochezia, hematuria, were reported. nerve pain or loss of motor function; signs
Immunogenicity (anti-dinutuximab anti- of low blood pressure such as confusion,
bodies) reported in 18% of pts. fainting, pallor; swelling of face, arms, or
legs. • Moderate to severe generalized

Canadian trade name Non-Crushable Drug High Alert drug


348 diphenhydrAMINE
pain is an expected side effect. Medications PRECAUTIONS
for pain, fever, and mild allergic reactions Contraindications: Hypersensitivity to di­-
will need to be provided before or during p­hen­hydrAMINE. Neonates or premature
each infusion; report any intolerance to infants, breastfeeding. Cautions: Narrow-
such medications. • Therapy is expected angle glaucoma, stenotic peptic ulcer, pros-
D to lower blood counts/immune system and tatic hypertrophy, pyloroduodenal/bladder
may increase risk of bleeding or infec- neck obstruction, asthma, COPD, increased
tion. • Drink plenty of fluids. • Treat- IOP, cardiovascular disease, hyperthyroid-
ment may be harmful to fetuses. Contracep- ism, elderly.
tion is recommended during therapy and
for at least 2 mos after discontinuation in ACTION
females of childbearing potential. Competes with histamine for H-1 recep-
tor site on effector cells in GI tract, blood
vessels, respiratory tract. Therapeutic
diphenhydrAMINE Effect: Produces anticholinergic, anti-
pruritic, antitussive, antiemetic, anti-
dye-fen-hye-dra-meen dyskinetic, sedative effects.
(Allerdryl , Banophen, Benadryl,
Benadryl Children’s Allergy, Diphen, PHARMACOKINETICS
Diphenhist, Genahist, Nytol) Route Onset Peak Duration
Do not confuse Benadryl with PO 15–30 min 1–4 hrs 4–6 hrs
benazepril, Bentyl, or Benylin, IV, IM Less than 1–4 hrs 4–6 hrs
or diphenhydrAMINE with 15 min
desipramine, dicyclomine, or
dimenhyDRINATE. Well absorbed after PO, parenteral
administration. Protein binding: 98%–
FIXED-COMBINATION(S) 99%. Widely distributed. Metabolized in
Advil PM: diphenhydramine/ibupro- liver. Primarily excreted in urine. Half-
fen (NSAID): 38 mg/200 mg. With life: 1–4 hrs. Adults: 7–12 hrs, elderly:
calamine, an astringent, and camphor, 9–18 hrs, children: 4–7 hrs.
a counterirritant (Caladryl).
LIFESPAN CONSIDERATIONS
uCLASSIFICATION
Pregnancy/Lactation: Crosses placenta.
PHARMACOTHERAPEUTIC: Hista- Detected in breast milk (may produce irri-
mine-1 antagonist, first generation. tability in breastfed infants). Increased risk
CLINICAL: Antihistamine, anticholiner- of seizures in neonates, premature infants
gic, antipruritic, antitussive, antiemetic, if used during third trimester of pregnancy.
antidyskinetic. May prohibit lactation. Children: Not rec-
ommended in newborns, premature infants
(increased risk of paradoxical reaction,
USES seizures). Elderly: Potentially inappropri-
Treatment of allergic reactions, including ate due to potent anticholinergic effects.
nasal allergies and allergic dermatoses; Increased risk for dizziness, sedation, con-
parkinsonism, including drug-induced fusion, hypotension, hyperexcitability.
extrapyramidal symptoms; prevention/
treatment of nausea, vomiting, or vertigo INTERACTIONS
due to motion sickness; antitussive; short- DRUG: Alcohol, other CNS depres-
term management of insomnia; adjunct to sants (e.g., LORazepam, morphine,
EPINEPHrine in treatment of anaphylaxis. zolpidem) may increase CNS depressant
Topical form used for relief of pruritus effects. Anticholinergics (e.g., acli-
from insect bites, skin irritations. dinium, ipratropium, tiotropium,
underlined – top prescribed drug
diphenhydrAMINE 349
umeclidinium) may increase anticho- Maximum: 400 mg/day. PO, IV, IM:
linergic effects. HERBAL: Gotu kola, CHILDREN: 5 mg/kg/day in divided doses
kava kava, valerian may increase CNS q6–8h. Maximum: 300 mg/day.
depression. FOOD: None known. LAB VAL-
UES: May suppress wheal/flare reactions to Motion Sickness
antigen skin testing unless drug is discontin- Note: When used for prophylaxis, give D
ued 4 days before testing. 30 min before motion.
PO: (Prophylaxis/Treatment): ADULTS,
AVAILABILITY (OTC) ELDERLY:25–50 mg q6–8h. CHILDREN: 5
Capsules: 25 mg, 50 mg. Cream: 1%, mg/kg/day in 3–4 divided doses. Maxi-
2%. Elixir: 12.5 mg/5 mL. Injection mum: 300 mg/day. IV/IM: (Treat-
Solution: 50 mg/mL. Liquid: 12.5 mg/5 ment): ADULTS, ELDERLY: 10–50 mg/
mL. Syrup: 12.5 mg/5 mL. Tablets: 25 dose. Maximum: 400 mg/day. CHIL-
mg, 50 mg. Tablets, Chewable: 12.5 mg. DREN: 5 mg/kg/day in 4 divided doses.
Maximum: 300 mg/day.
ADMINISTRATION/HANDLING
Antitussive
IV PO: ADULTS, ELDERLY, CHILDREN 12 YRS
• May be given undiluted. • Give IV AND OLDER: 25 mg q4h. Maximum:
injection over at least 1 min. Maximum 150 mg/day.
rate: 25 mg/min. Nighttime Sleep Aid
IM PO: ADULTS, ELDERLY, CHILDREN 12 YRS
• Give deep IM into large muscle mass. AND OLDER: 25–50mg at bedtime. CHIL-
DREN 2–11 YRS: 1mg/kg/dose. Maxi-
PO mum Single Dose: 50 mg.
• Give with food to decrease GI dis-
tress. • Scored tablets may be crushed. Pruritus
Topical: ADULTS, ELDERLY, CHILDREN 12
IV INCOMPATIBILITIES YRS AND OLDER: Apply 1% or 2% cream
Allopurinol (Aloprim), cefepime (Maxi- or spray 3–4 times/day. CHILDREN 2–11
pime), dexamethasone (Decadron), fos- YRS: Apply 1% cream or spray 3–4
carnet (Foscavir). times/day.

IV COMPATIBILITIES Parkinsonism
PO: ADULTS, ELDERLY: 25–50 mg 3–4
Atropine, cisplatin (Platinol), cyclo-
phosphamide (Cytoxan), cytarabine times/day. IM/IV: 10–50 mg/dose up to
(Ara-C), fentaNYL, glycopyrrolate (Rob- 100 mg/dose. Maximum: 400 mg/day.
inul), heparin, hydrocortisone (SOLU- Dosage in Renal/Hepatic Impairment
Cortef), HYDROmorphone (Dilaudid), No dose adjustment.
hydrOXYzine (Vistaril), lidocaine,
metoclopramide (Reglan), ondanse- SIDE EFFECTS
tron (Zofran), potassium chloride, Frequent: Drowsiness, dizziness, muscle
promethazine (Phenergan), propofol weakness, hypotension, urinary reten-
(Diprivan). tion, thickening of bronchial secretions,
INDICATIONS/ROUTES/DOSAGE dry mouth, nose, throat, lips; in elderly:
sedation, dizziness, hypotension. Occa-
Allergic Reaction
sional: Epigastric distress, flushing,
25–50 mg q4–8h.
PO: ADULTS, ELDERLY:
visual/hearing disturbances, paresthesia,
Maximum: 300 mg/day. IM, IV: diaphoresis, chills.
10–50 mg/dose up to 100 mg/dose.

Canadian trade name Non-Crushable Drug High Alert drug


350 diphenoxylate with atropine

ADVERSE EFFECTS/TOXIC FIXED-COMBINATION(S)


REACTIONS Lomotil: diphenoxylate/atropine (anti­
Hypersensitivity reactions (eczema, pruri- cholinergic, antispasmodic): 2.5 mg/
tus, rash, cardiac disturbances, photosen- 0.025 mg.
sitivity) may occur. Overdose symptoms
D may vary from CNS depression (sedation, uCLASSIFICATION
apnea, hypotension, cardiovascular col- PHARMACOTHERAPEUTIC: Opioid/
lapse, death) to severe paradoxical reac- anticholinergic (Schedule V). CLIN-
tions (hallucinations, tremors, seizures). ICAL: Antidiarrheal.
Children, infants, neonates may experi-
ence paradoxical reactions (restlessness,
insomnia, euphoria, nervousness, trem- USES
ors). Overdosage in children may result in Adjunctive treatment of acute, chronic
hallucinations, seizures, death. diarrhea.
NURSING CONSIDERATIONS PRECAUTIONS
BASELINE ASSESSMENT
Contraindications: Hypersensitivity to
di­phe­noxy­late, atropine. Obstructive jaundice,
If pt is having acute allergic reaction, obtain diarrhea associated with pseudomembra-
history of recently ingested foods, drugs, nous colitis or enterotoxin-producing bacte-
environmental exposure, emotional stress. ria. Cautions: Children (not recommended
Monitor B/P rate; depth, rhythm, type of in children younger than 2 yrs): acute ulcer-
respiration; quality, rate of pulse. Assess ative colitis, renal/hepatic impairment.
lung sounds for rhonchi, wheezing, rales.
INTERVENTION/EVALUATION
ACTION
Monitor B/P, esp. in elderly (increased Acts locally and centrally on gastric
risk of hypotension). Monitor children mucosa. Therapeutic Effect: Reduces
closely for paradoxical reaction. Monitor excessive GI motility and GI propulsion.
for sedation. PHARMACOKINETICS
PATIENT/FAMILY TEACHING Onset Peak Duration
• Tolerance to antihistaminic effect gen- Antidiar- 45–60 — 3–4 hrs
erally does not occur; tolerance to sedative rheal min
effect may occur. • Avoid tasks that re-
quire alertness, motor skills until response Well absorbed from GI tract. Metabolized
to drug is established. • Dry mouth, in liver. Primarily eliminated in feces.
drowsiness, dizziness may be an expected Half-life: 2.5 hrs; metabolite: 12–24 hrs.
response to drug. • Avoid alcohol. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if drug
crosses placenta or is distributed in breast
diphenoxylate with milk. Children: Not recommended
(increa­sed susceptibility to toxicity, includ-
atropine ing respiratory depression). Elderly: More
susceptible to anticholinergic effects, confu-
dye-fen-ox-i-late at-roe-peen sion, respiratory depression.
(Lomotil)
Do not confuse Lomotil with INTERACTIONS
LaMICtal, LamISIL, Lamotrigine, DRUG: Alcohol, other CNS depres-
Lanoxin, or Lasix sants (e.g., LORazepam, morphine,
zolpidem) may increase CNS depressant

underlined – top prescribed drug


DOBUTamine 351
effects. Anticholinergics (e.g., acli- vomiting) occur rarely. Severe anticholin-
dinium, ipratropium, tiotropium, ergic reaction (severe lethargy, hypotonic
umeclidinium) may increase effects of reflexes, hyperthermia) may result in
atropine. MAOIs (e.g., phenelzine, severe respiratory depression, coma.
selegiline) may precipitate hypertensive
crisis. HERBAL: Herbals with seda- NURSING CONSIDERATIONS D
tive properties (e.g., chamomile, BASELINE ASSESSMENT
kava kava, valerian) may increase CNS
depression. FOOD: None known. LAB Check baseline hydration status: skin tur-
VALUES: May increase serum amylase.
gor, mucous membranes for dryness, uri-
nary status. Assess usual stool frequency,
AVAILABILITY (Rx) consistency.
2.5 mg diphenoxylate/
Liquid: (Lomotil): INTERVENTION/EVALUATION
0.025 mg atropine/5 mL. Tablets: (Lomo- Encourage adequate fluid intake. Assess
til): 2.5 mg diphenoxylate/0.025 mg bowel sounds for peristalsis. Monitor daily
atropine. pattern of bowel activity, stool consistency.
ADMINISTRATION/HANDLING Record time of evacuation. Assess for ab-
dominal disturbances. Discontinue medi-
PO cation if abdominal distention occurs.
• Give without regard to food. If GI irrita-
tion occurs, give with food. • Use liquid for PATIENT/FAMILY TEACHING
children 2–12 yrs (use graduated dropper • Avoid tasks that require alertness, mo-
for administration of liquid medication). tor skills until response to drug is estab-
lished. • Avoid alcohol. • Report
INDICATIONS/ROUTES/DOSAGE persistent fever, palpitations, diarrhea.
Diarrhea • Report abdominal distention.
PO: ADULTS, ELDERLY: Initially, 5 mg (2
tabs or 10 mL) 3–4 times/day. Maxi-
mum: 20 mg/day. Then reduce dose as
needed. CHILDREN: 0.3–0.4 mg/kg/day DOBUTamine
in 4 divided doses (Maximum: 10 mg/
day); then reduce dose as needed. doe-bue-ta-meen
(Dobutrex )
Dosage in Renal/Hepatic Impairment Do not confuse DOBUTamine
No dose adjustment. Use caution with with DOPamine.
severe renal/hepatic disease.
uCLASSIFICATION
SIDE EFFECTS PHARMACOTHERAPEUTIC: Adrenergic
Frequent: Drowsiness, light-headedness, agonist. CLINICAL: Cardiac stimulant.
dizziness, nausea. Occasional: Head-
ache, dry mouth. Rare: Flushing, tachy-
USES
cardia, urinary retention, constipation,
paradoxical reaction (marked by rest- Short-term management of cardiac
lessness, agitation), blurred vision. decompensation.

ADVERSE EFFECTS/TOXIC PRECAUTIONS


REACTIONS Contraindications: Hypersensitivity to
Dehydration may predispose pt to dobutamine. Hypertrophic cardiomy-
diphenoxylate toxicity. Paralytic ileus, opathy with outflow obstruction. Cau-
tions: Atrial fibrillation, hypovolemia,
toxic megacolon (constipation, decreased
appetite, abdominal pain with nausea/ post-MI, concurrent use of MAOIs, elderly.

Canadian trade name Non-Crushable Drug High Alert drug


352 DOBUTamine

ACTION (due to oxidation) does not indicate signifi-


Direct-action inotropic agent act- cant loss of potency if used within recom-
ing primarily on myocardial beta1- mended time period. • Further diluted
adrenergic receptors. Therapeutic solution for infusion is stable for 48 hrs at
Effect: Enhances myocardial contractil- room temperature, 7 days if refrigerated.
D ity, increases heart rate.
IV INCOMPATIBILITIES
PHARMACOKINETICS Acyclovir (Zovirax), alteplase (Activase),
Route Onset Peak Duration amphotericin B complex (Abelcet, AmBi-
IV 1–2 min 10 min Length of infusion some, Amphotec), bumetanide (Bumex),
cefepime (Maxipime), foscarnet (Foscavir),
Metabolized in liver. Primarily excreted furosemide (Lasix), heparin, piperacillin/
in urine. Not removed by hemodialysis. tazobactam (Zosyn), sodium bicarbonate.
Half-life: 2 min.
IV COMPATIBILITIES
LIFESPAN CONSIDERATIONS Amiodarone (Cordarone), calcium
Pregnancy/Lactation: Unknown if drug chloride, calcium gluconate, dilTIAZem
crosses placenta or is distributed in (Cardizem), DOPamine (Intropin), enal-
breast milk. Children/Elderly: No age- april (Vasotec), EPINEPHrine, famotidine
related precautions noted. (Pepcid), HYDROmorphone (Dilaudid),
insulin (regular), lidocaine, LORazepam
INTERACTIONS (Ativan), magnesium sulfate, midazolam
DRUG: Sympathomimetics (e.g., nor­ (Versed), milrinone (Primacor), mor-
epinephrine, phenylephrine) may phine, nitroglycerin, nitroprusside
increase effects. HERBAL: None sig- (Nipride), norepinephrine (Levophed),
nificant. FOOD: None known. LAB VAL- potassium chloride, propofol (Diprivan).
UES: May decrease serum potassium.
INDICATIONS/ROUTES/DOSAGE
AVAILABILITY (Rx) b ALERT c Dosage determined by se-
Infusion (Ready-to-Use): 1 mg/mL (250 verity of decompensation.
mL), 2 mg/mL (250 mL), 4 mg/mL (250
mL). Injection Solution: 12.5-mg/mL vial. Cardiac Decompensation (Hemodynamic
Support)
ADMINISTRATION/HANDLING IV infusion: ADULTS, ELDERLY: Initially,
b ALERT c Correct hypovolemia with 0.5–2.5 mcg/kg/min. Maintenance: 2–20
volume expanders before DOBUTamine mcg/kg/min titrated to desired response. May
infusion. Pts with atrial fibrillation should be infused at a rate of up to 40 mcg/kg/min to
be digitalized before infusion. Administer increase cardiac output. NEONATES, INFANTS,
by IV infusion only. CHILDREN, ADOLESCENTS: Initially, 0.5–1 mcg/
kg/min. Titrate gradually every few minutes
IV
until desired response. Usual Range: 2–20
Reconstitution • Dilute vial in 0.9% mcg/kg/minute.
NaCl or D5W to maximum concentration
Dosage in Renal/Hepatic Impairment
of 5,000 mcg/mL (5 mg/mL).
No dose adjustment.
Rate of administration • Use infusion
pump to control flow rate. • Titrate dosage SIDE EFFECTS
to individual response. • Infiltration causes
Frequent (greater than 5%): Increased heart
local inflammatory changes. • Extravasa-
rate, B/P. Occasional (5%–3%): Pain at injec-
tion may cause dermal necrosis.
tion site. Rare (3%–1%): Nausea, headache,
Storage • Store at room tempera-
anginal pain, shortness of breath, fever.
ture. • Pink discoloration of solution

underlined – top prescribed drug


DOCEtaxel 353

ADVERSE EFFECTS/TOXIC Do not confuse DOCEtaxel with


REACTIONS PACLitaxel or Taxotere with
Overdose may produce severe tachycar- Taxol.
dia, severe hypertension. uCLASSIFICATION
NURSING CONSIDERATIONS PHARMACOTHERAPEUTIC: Antimi- D
crotubular, taxoid. CLINICAL: Anti-
BASELINE ASSESSMENT neoplastic.
Pt must be on continuous cardiac moni-
toring. Determine weight (for dosage cal-
culation). Obtain initial B/P, heart rate, USES
respirations. Correct hypovolemia before Treatment of locally advanced or meta-
drug therapy. static breast carcinoma after failure
INTERVENTION/EVALUATION
of prior chemotherapy. Treatment of
metastatic non–small-cell lung cancer
Continuously monitor for cardiac rate, (NSCLC). Treatment of metastatic pros-
arrhythmias. Maintain accurate I&O; tate cancer, head and neck cancer (with
measure urinary output frequently. Assess predniSONE). Treatment of advanced
serum potassium, plasma DOBUTamine gastric adenocarcinoma. OFF-LABEL:
(therapeutic range: 40–190 ng/mL). Mon- Bladder, esophageal, ovarian, small-cell
itor B/P continuously (hypertension risk lung carcinoma; soft tissue carcinoma,
greater in pts with preexisting hyperten- cervical cancer, Ewing’s sarcoma,
sion). Check cardiac output, pulmonary osteosarcoma.
wedge pressure/central venous pressure
(CVP) frequently. Immediately notify phy- PRECAUTIONS
sician of decreased urinary output, cardiac Contraindications: Hypersensitivity to
arrhythmias, significant increase in B/P, DOCEtaxel. History of severe hypersensi-
heart rate, or less commonly, hypotension. tivity to drugs formulated with polysorbate
80, neutrophil count less than 1,500 cells/
mm3. Cautions: Hepatic impairment,
DOCEtaxel myelosuppression, concomitant CYP3A4
inhibitors/inducers, fluid retention, pul-
doe-se-tax-el monary disease, HF, active infection.
(Taxotere)
ACTION
j BLACK BOX ALERT jAvoid
use with serum bilirubin more Promotes assembly of microtubules and
than upper limit of normal (ULN) or inhibits depolymerization of tubulin,
serum ALT, AST more than 1.5 times which stabilizes microtubules. Thera-
ULN in conjunction with serum
alkaline phosphatase more than 2.5 peutic Effect: Inhibits DNA, RNA, pro-
times ULN. Severe hypersensitiv- tein synthesis.
ity reaction (rash, hypotension,
bronchospasm, anaphylaxis) may PHARMACOKINETICS
occur. Fluid retention syndrome Widely distributed. Protein binding: 94%.
(pleural effusions, ascites, edema,
dyspnea at rest) has been reported. Extensively metabolized in liver. Excreted
Pts with abnormal hepatic function, in feces (75%), urine (6%). Half-
receiving higher doses, and pts life: 11.1 hrs.
with non–small-cell lung carcinoma
(NSCLC) and history of prior plati- LIFESPAN CONSIDERATIONS
num treatment receiving DOCEtaxel
dose of 100 mg/m2 at higher risk for Pregnancy/Lactation: May cause fetal
mortality. Avoid use with ANC less harm. Unknown if distributed in breast
than 1,500 cells/mm3. milk. Breastfeeding not recommended.

Canadian trade name Non-Crushable Drug High Alert drug


354 DOCEtaxel
Children: Safety and efficacy not (do not store in PVC bags). • Diluted
established in pts younger than 16 yrs. solution should be used within 4 hrs
Elderly: No age-related precautions noted. (including infusion time).
INTERACTIONS IV INCOMPATIBILITIES
D DRUG: Strong CYP3A4 inhibitors Amphotericin B (Fungizone), methyl-
(e.g., clarithromycin, ketoconazole, PREDNISolone (SOLU), nalbuphine
ritonavir) may increase concentra- (Nubain).
tion/effect. Strong CYP3A4 inducers
(e.g., carBAMazepine, phenytoin, IV COMPATIBILITIES
rifAMPin) may decrease concentration/ Bumetanide (Bumex), calcium glu-
effect. Live virus vaccines may poten- conate, dexamethasone (Decadron),
tiate replication, increase vaccine side diphenhydrAMINE (Benadryl), DOBUTa-
effects, decrease pt’s antibody response mine (Dobutrex), DOPamine (Intropin),
to vaccine. HERBAL: Echinacea may furosemide (Lasix), granisetron (Kytril),
decrease concentration. St. John’s heparin, HYDROmorphone (Dilaudid),
wort may decrease concentration/effect. LORazepam (Ativan), magnesium sul-
FOOD: None known. LAB VALUES: May fate, mannitol, morphine, ondansetron
increase serum alkaline phosphatase, (Zofran), palonosetron (Aloxi), potas-
bilirubin, ALT, AST. Reduces neutrophil, sium chloride.
platelet count, Hgb, Hct.
INDICATIONS/ROUTES/
AVAILABILITY (Rx) DOSAGE
Injection, Powder for Reconstitution: 20 b ALERT c Pt should be premedicated
mg, 80 mg. Injection Solution: 10 mg/ with oral corticosteroids (e.g., dexa-
mL, 20 mg/mL. methasone 16 mg/day for 5 days begin-
ning day 1 before DOCEtaxel therapy);
ADMINISTRATION/HANDLING reduces severity of fluid retention, hyper-
IV sensitivity reaction.
Reconstitution (solution) • Withdraw Breast Carcinoma
dose and add to 250–500 mL 0.9% NaCl IV: ADULTS: Locally advanced or meta-
or D5W in glass or polyolefin container to static: 60–100 mg/m2 given over 1 hr
provide a final concentration of 0.3–0.74 q3wks as a single agent. Operable, node
mg/mL. (Powder) • Add 1 mL dilu- positive: 75 mg/m2 q3wks for 6 courses
ent provided to 20-mg vial to provide a (in combination with DOXOrubicin and
concentration of 20 mg/0.8 mL (4 mL to cyclophosphamide).
80-mg vial to provide a concentration of
24 mg/mL). Shake well. Further dilute in Non–Small-Cell Lung Carcinoma
250 mL NaCl or D5W to a final concentra- IV: ADULTS: 75 mg/m2 q3wks (as
tion of 0.3–0.74 mg/mL. monotherapy or in combination with
Rate of administration • Administer CISplatin).
as a 1-hr infusion. • Monitor closely
for hypersensitivity reaction (flushing, Prostate Cancer
localized skin reaction, bronchospasm IV: ADULTS, ELDERLY: 75 mg/m2 q3wks
[may occur within a few min after begin- with concurrent administration of
ning infusion]). predniSONE.
Storage • Store vials between 36°
F–77°F. • Protect from bright light. Head/Neck Cancer
• If refrigerated, stand vial at room tem- 75 mg/m2 q3wks
IV: ADULTS, ELDERLY:
perature for 5 min before administering (in combination with CISplatin and

underlined – top prescribed drug


DOCEtaxel 355
fluorouracil) for 3–4 cycles, followed by Gastric or Head and Neck Cancer
radiation therapy. Reduce dose to 60 mg/m2; if neutropenic
toxicity persists, further reduce to 45 mg/
Gastric Adenocarcinoma m2. For Grade 3 or 4 thrombocytopenia,
mg/m2 q3wks
IV: ADULTS, ELDERLY: 75 reduce dose from 75 mg/m2 to 60 mg/
(in combination with CISplatin and m2; discontinue if toxicity persists. D
fluorouracil).
Dosage in Renal Impairment
Dose Modification for Gastric or Head/ No dose adjustment.
Neck Cancer
Dosage in Hepatic Impairment
ALT, AST 2.5 to 5 times 80% of dose
ULN and alkaline Total bilirubin more than ULN, or
phosphatase less than or ALT, AST more than 1.5 times ULN
equal to 2.5 times ULN with alkaline phosphatase more than
ALT, AST 1.5 to 5 times ULN 80% of dose 2.5 times ULN: Use not recommended.
and alkaline phosphatase
2.5 to 5 times ULN SIDE EFFECTS
ALT, AST greater than 5 Discontinue Frequent (80%–19%): Alopecia, asthenia,
times ULN and/or alkaline DOCEtaxel hypersensitivity reaction (e.g., dermatitis),
phosphatase greater than which is decreased in pts pretreated with
5 times ULN
oral corticosteroids; fluid retention, stoma-
Note: Toxicity includes febrile neutro- titis, nausea, diarrhea, fever, nail changes,
penia, neutrophils less than 500 cells/ vomiting, myalgia. Occasional: Hypoten-
mm3 for longer than 1 wk, severe cuta- sion, edema, anorexia, headache, weight
neous reactions. Also, for NSCLC, platelet gain, infection (urinary tract, injection
nadir less than 25,000 cells/mm3, any site, indwelling catheter tip), dizziness.
CTCAE Grade 3 or 4 nonhematologic Rare: Dry skin, sensory disorders (vision,
toxicity. speech, taste), arthralgia, weight loss, con-
junctivitis, hematuria, proteinuria.
Breast Cancer
Reduce dose to 75 mg/m2; if toxicity per- ADVERSE EFFECTS/TOXIC
sists, reduce to 55 mg/m2. REACTIONS
In pts with normal hepatic function,
Breast Cancer Adjuvant neutropenia (ANC count less than 1,500
Administer when neutrophils are less cells/mm3), leukopenia (WBC count less
than 1,500 cells/mm3. If toxicity persists, than 4,000 cells/mm3) occur in 96% of
or Grade 3 or 4 stomatitis, reduce dose pts; anemia (hemoglobin level less than
to 60 mg/m2. 11 g/dL) occurs in 90% of pts; throm-
bocytopenia (platelet count less than
Non–Small-Cell Lung Cancer 100,000 cells/mm3) occurs in 8% of pts;
Monotherapy infection occurs in 28% of pts. Neuro-
Hold dose until toxicity resolves, then sensory, neuromotor disturbances (distal
reduce dose to 55 mg/m2. Discontinue if paresthesia, weakness) occur in 54%
Grade 3 or 4 neuropathy occurs. and 13% of pts, respectively.
Combination Therapy
Reduce dose to 65 mg/m2; may further NURSING CONSIDERATIONS
reduce to 50 mg/m2 if needed.
BASELINE ASSESSMENT
Prostate Cancer Obtain baseline ANC, CBC, serum chem-
Reduce dose to 60 mg/m2; discontinue if istries. Offer emotional support to pt,
toxicity persists. family. Antiemetics may be effective in
preventing, treating nausea/vomiting.

Canadian trade name Non-Crushable Drug High Alert drug


356 dofetilide
Pt should be pretreated with corticoste- NSR. Conversion of atrial fibrillation/flut-
roids to reduce fluid retention, hypersen- ter to NSR.
sitivity reaction.
PRECAUTIONS
INTERVENTION/EVALUATION
Contraindications: Hypersensitivity to
D Frequently monitor blood counts, par- dofetilide. Congenital or acquired pro-
ticularly ANC count (less than 1,500 longed QT syndrome (do not use if base-
cells/mm3 requires discontinuation of line QT interval or QTc is greater than
therapy). Monitor LFT, serum uric acid 440 msec), severe renal impairment,
levels. Observe for cutaneous reactions concurrent use of drugs that may pro-
(rash with eruptions, mainly on hands, long QT interval, hypokalemia, hypomag-
feet). Assess for extravascular fluid ac- nesemia, concurrent use with verapamil,
cumulation: rales in lungs, dependent dolutegravir, itraconazole, ketoconazole,
edema, dyspnea at rest, pronounced ab- prochlorperazine, megestrol, cimetidine,
dominal distention (due to ascites). hydroCHLOROthiazide, trimethoprim.
PATIENT/FAMILY TEACHING Severe renal impairment (CrCl less than
20 mL/min). Cautions: Severe hepatic
• Hair loss is reversible, but new hair impairment, renal impairment, pts pre-
growth may have different color or tex- viously taking amiodarone, elderly. Con-
ture. • New hair growth resumes 2–3 current use of other agents that prolong
mos after last therapy dose. • Main- QT interval. Pts with sick sinus syndrome
tain strict oral hygiene. • Do not have or second- or third-degree heart block
immunizations without physician’s ap- unless functional pacemaker in place.
proval (drug lowers resistance). • Avoid
those who have recently taken any live vi- ACTION
rus vaccine. • Report persistent nausea, Prolongs repolarization without affect-
diarrhea, respiratory difficulty, chest pain, ing conduction velocity by blocking
fever, chills, unusual bleeding, bruising. one or more time-dependent potassium
currents. No effect on sodium chan-
nels, alpha-adrenergic, beta-adrenergic
dofetilide receptors. Therapeutic Effect: Termi-
nates reentrant tachyarrhythmias, pre-
doe-fet-i-lide venting reinduction.
(Tikosyn)
j BLACK BOX ALERT jPt PHARMACOKINETICS
must be placed in a setting with Well absorbed following PO admin-
continuous cardiac monitoring for istration. 80% eliminated in urine as
minimum of 3 days and monitored
by staff familiar with treatment of unchanged drug, 20% excreted as mini-
life-threatening arrhythmias. mally active metabolites. Protein binding:
60%–70%. Half-life: 2–3 hrs.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Potassi-
LIFESPAN CONSIDERATIONS
um channel blocker. CLINICAL: An- Pregnancy/Lactation: Unknown if
tiarrhythmic: Class III. drug is distributed in breast milk. Chil-
dren: No age-related precautions noted.
Elderly: Age-related renal impairment
USES may require dosage adjustment.
Maintenance of normal sinus rhythm
(NSR) in pts with chronic atrial fibril- INTERACTIONS
lation/atrial flutter of longer than 1-wk DRUG: Cimetidine, lamotrigine, keto-
duration who have been converted to conazole, trimethoprim, verapamil

underlined – top prescribed drug


donepezil 357
may increase concentration/effect. May NURSING CONSIDERATIONS
increase QT interval-prolonging effect of
citalopram, clarithromycin, erythro- BASELINE ASSESSMENT
mycin, fingolimod, hydrochlorothia- Assess baseline serum electrolytes (esp.
zide, levofloxacin, ribociclib. HERBAL: potassium, magnesium). Prior to initi-
None significant. Ephedra may worsen ating treatment, QTc intervals must be D
arrhythmias. FOOD: None known. LAB determined. Do not use if heart rate less
VALUES: None significant. than 50 beats/min. Provide continuous
ECG monitoring, calculation of creatinine
AVAILABILITY (Rx) clearance, equipment for resuscitation
Capsules: 125 mcg, 250 mcg, 500 mcg. available for minimum of 3 days. Antici-
pate proarrhythmic events.
ADMINISTRATION/HANDLING
PO INTERVENTION/EVALUATION
• Give without regard to food. • Do Assess for conversion of cardiac dys-
not break, crush, or open capsules. rhythmias and absence of new arrhyth-
mias. Constantly monitor ECG. Provide
INDICATIONS/ROUTES/DOSAGE emotional support. Monitor renal func-
b ALERT c ECG interval measurements tion for electrolyte imbalance (prolonged
(esp. Qtc intervals), creatinine clear- or excessive diarrhea, sweating, vomit-
ance, must be determined prior to first ing, thirst).
dose. Correct hypokalemia, hypomagne-
semia prior to starting. PATIENT/FAMILY TEACHING
• Instruct pt on need for compliance
Antiarrhythmias and requirement for periodic monitoring
PO: ADULTS, ELDERLY: Initially, 500 mcg of ECG and renal function. • Do not
twice daily. Modify dose in response to break, crush, or open capsule.
QTc interval.
Dosage in Renal Impairment
Creatinine
Clearance Dosage
donepezil
Greater than 500 mcg twice daily
doe-nep-e-zil
60 mL/min
40–60 mL/min 250 mcg twice daily (Aricept RDT , Aricept)
20–39 mL/min 125 mcg twice daily Do not confuse Aricept with
Less than Contraindicated Aciphex, Ascriptin, or Azilect.
20 mL/min
FIXED-COMBINATION(S)
Dosage in Hepatic Impairment Namzaric: donepezil/memantine
No dose adjustment. (NMDA receptor antagonist): 10
mg/14 mg, 10 mg/28 mg.
SIDE EFFECTS
Rare (less than 2%): Headache, chest uCLASSIFICATION
pain, dizziness, dyspnea, nausea, insom- PHARMACOTHERAPEUTIC: Central
nia, back/abdominal pain, diarrhea, rash. acetylcholinesterase inhibitor. CLINI-
CAL: Cholinergic.
ADVERSE EFFECTS/TOXIC
REACTIONS
Angioedema, bradycardia, cerebral isch- USES
emia, facial paralysis, serious arrhyth- Treatment of mild, moderate, or severe
mias (ventricular, various forms of dementia of Alzheimer’s disease.
block) have been noted. OFF-LABEL: Treatment of behavioral

Canadian trade name Non-Crushable Drug High Alert drug


358 donepezil
syndromes in dementia, dementia associ- ADMINISTRATION/HANDLING
ated with Parkinson’s disease, Lewy body PO
dementia. • May be given at bedtime without
regard to food. • Swallow tablets
PRECAUTIONS
whole; do not break, crush, dissolve, or
D Contraindications: History of hypersen- divide. • Follow dose with water.
sitivity to donepezil, other piperidine
derivatives. Cautions: Asthma, COPD, INDICATIONS/ROUTES/
bradycardia, bladder outflow obstruc- DOSAGE
tion, history of ulcer disease, those
Alzheimer’s Disease
taking concurrent NSAIDs, supraven-
PO: ADULTS, ELDERLY: For mild to mod-
tricular cardiac conduction distur-
erate, initially 5 mg/day at bedtime. May
bances (e.g., “sick sinus syndrome,”
increase at 4- to 6-wk intervals to 10
Wolff-Parkinson-White syndrome),
mg/day at bedtime. Range: 5–10 mg/
seizure disorder.
day. For moderate to severe Alzheim-
ACTION er’s, a dose of 23 mg once daily can be
administered once pt has been taking 10
Reversibly inhibits enzyme acetylcho-
mg once daily for at least 3 mos. Range:
linesterase, increasing concentration of
10–23 mg/day.
acetylcholine at cholinergic synapses,
enhancing cholinergic function in CNS.
Dosage in Renal/Hepatic Impairment
Therapeutic Effect: Slows progression
No dose adjustment.
of Alzheimer’s disease.
PHARMACOKINETICS SIDE EFFECTS
Well absorbed after PO administration. Frequent (11%–8%): Nausea, diarrhea,
Protein binding: 96%. Extensively metab- headache, insomnia, nonspecific pain,
olized. Eliminated in urine, feces. Half- dizziness. Occasional (6%–3%): Mild mus-
life: 70 hrs. cle cramps, fatigue, vomiting, anorexia,
ecchymosis. Rare (3%–2%): Depression,
LIFESPAN CONSIDERATIONS abnormal dreams, weight loss, arthritis,
Pregnancy/Lactation: Unknown if drug drowsiness, syncope, frequent urination.
is distributed in breast milk. Chil-
dren: Safety and efficacy not established. ADVERSE EFFECTS/TOXIC
Elderly: No age-related precautions REACTIONS
noted. Overdose may result in cholinergic cri-
sis (severe nausea, increased salivation,
INTERACTIONS diaphoresis, bradycardia, hypotension,
DRUG: Anticholinergic agents (e.g., flushed skin, abdominal pain, respiratory
glycopyrrolate, scopolamine) may depression, seizures, cardiorespiratory
decrease therapeutic effect. May increase collapse). Increasing muscle weakness
concentration/effects of antipsychotic may occur, resulting in death if muscles
agents, beta blockers (e.g., ateno- of respiration become involved. Antidote:
lol, carvedilol, metoprolol), succi- Atropine sulfate 1–2 mg IV with subsequent
nylcholine. HERBAL: None significant. doses based on therapeutic response.
FOOD: None known. LAB VALUES: None
significant. NURSING CONSIDERATIONS
BASELINE ASSESSMENT
AVAILABILITY (Rx)
Assess cognitive function (e.g., memory,
Tablets: 5 mg, 10 mg, 23 mg. Tablets
attention, reasoning). Obtain baseline
(Orally Disintegrating): 5 mg, 10 mg.

underlined – top prescribed drug


DOPamine 359
vital signs. Assess history for peptic ul- PRECAUTIONS
cer, urinary obstruction, asthma, COPD, Contraindications: Hypersensitivity to do­
seizure disorder, cardiac conduction dis- pamine, sulfites. Pheochromocytoma, ventric-
turbances. ular fibrillation. Uncorrected tachyar­rhythmias.
INTERVENTION/EVALUATION Cautions: Ischemic heart disease, occlusive
vascular disease, hypovolemia, recent use of D
Monitor behavior, mood/cognitive func-
MAOIs (within 2–3 wks), ventricular arrhyth-
tion, activities of daily living. Monitor
mias, post-MI.
for cholinergic reaction (GI discomfort/
cramping, feeling of facial warmth, exces- ACTION
sive salivation/diaphoresis), lacrimation,
Stimulates adrenergic and dopami-
pallor, urinary urgency, dizziness. Monitor
nergic receptors. Effects are dose
for nausea, diarrhea, headache, insomnia.
dependent. Lower dosage stimulates
PATIENT/FAMILY TEACHING dopaminergic receptors, causing renal
• Report nausea, vomiting, diarrhea, vasodilation. Higher doses stimu-
diaphoresis, increased salivary secre- late both dopaminergic and beta1-
tions, severe abdominal pain, dizzi- adrenergic receptors, causing cardiac
ness. • May take without regard to food stimulation and renal vasodilation.
(best taken at bedtime). • Not a cure Higher doses stimulate alpha-adren-
for Alzheimer’s disease but may slow ergic receptors, causing vasoconstric-
progression of symptoms. tion, increased B/P. Therapeutic
Effect: Low dosage (1–5 mcg/kg/
min): Increases renal blood flow, uri-
nary flow, sodium excretion. Low to
DOPamine moderate dosage (5–10 mcg/kg/
min): Increases myocardial contractil-
dope-a-meen ity, stroke volume, cardiac output. High
j BLACK BOX ALERT jIf extrava- dosage (greater than 10 mcg/kg/
sation occurs, infiltrate area with min): Increases peripheral resistance,
phentolamine (5–10 mL 0.9% NaCl) vasoconstriction, B/P.
as soon as possible, no later than
12 hrs after extravasation. PHARMACOKINETICS
Do not confuse DOPamine with Route Onset Peak Duration
DOBUTamine or Dopram. IV 1–2 min N/A Less than
uCLASSIFICATION 10 min

PHARMACOTHERAPEUTIC: Sympa- Widely distributed. Does not cross


thomimetic (adrenergic agonist). blood-brain barrier. Metabolized in liver,
CLINICAL: Cardiac stimulant, vaso- kidneys, plasma. Primarily excreted in
pressor. urine. Not removed by hemodialysis.
Half-life: 2 min.
USES LIFESPAN CONSIDERATIONS
Adjunct in treatment of shock (e.g., MI, Pregnancy/Lactation: Unknown if
trauma, renal failure, cardiac decompen- drug crosses placenta or is distributed in
sation, open heart surgery), persisting breast milk. Children: Recommended
after adequate fluid volume replacement. close hemodynamic monitoring (gan-
OFF-LABEL: Symptomatic bradycardia or grene due to extravasation reported).
heart block unresponsive to atropine or Elderly: No age-related precautions
cardiac pacing. noted.

Canadian trade name Non-Crushable Drug High Alert drug


360 DOPamine

INTERACTIONS (Dobutrex), enalapril (Vasotec), EPINEPH-


DRUG: Ergot derivatives (e.g., ergot- rine, heparin, HYDROmorphone (Dilau-
amine), MAOIs (e.g., phenelzine, did), labetalol (Trandate), levoFLOXacin
selegiline), tricyclic antidepressants (Levaquin), lidocaine, LORazepam (Ati-
(e.g., amitriptyline) may increase van), methylPREDNISolone (Solu-Medrol),
D hypertensive effects. May increase hypoten- midazolam (Versed), milrinone (Prima-
sive effect of lurasidone. HERBAL: None cor), morphine, niCAR­dipine (Cardene),
significant. FOOD: None known. LAB VAL- nitroglycerin, norepinephrine (Levophed),
UES: None significant. piperacillin/tazobactam (Zosyn), potas-
sium chloride, propofol (Diprivan).
AVAILABILITY (Rx)
INDICATIONS/ROUTES/DOSAGE
Injection Solution: 40 mg/mL, 80 mg/
mL, 160 mg/mL. Injection (Premix with b ALERT c    Effects of DOPamine are
Dextrose): 0.8 mg/mL (250 mL, 500 dose dependent. Titrate to desired re-
mL), 1.6 mg/mL (250 mL, 500 mL), 3.2 sponse. Doses greater than 20 mcg/kg/min
mg/mL (250 mL). may not have beneficial effect on BP and
may increase risk of tachyarrhythmias.
ADMINISTRATION/HANDLING
Hemodynamic Support
b ALERT c Fluid volume depletion
IV infusion: ADULTS, ELDERLY, CHIL-
must be corrected before administering
DREN: Range: 2–20 mcg/kg/min. Titrate to
DOPamine (may be used concurrently
desired response. May gradually increase
with fluid replacement).
by 5–10 mcg/kg/min increments. Maxi-
IV mum: 50 mcg/kg/min. NEONATES: 2–20
mcg/kg/min. Titrate gradually by 5–10
Reconstitution • Available prediluted in mcg/kg/min to desired response.
250 or 500 mL D5W or dilute in 250–500
mL 0.9% NaCl or D5W, to maximum con- SIDE EFFECTS
centration of 3,200 mcg/mL (3.2 mg/mL). Frequent: Headache, arrhythmias, tachy­
Rate of administration • Administer cardia, anginal pain, palpitations,
into large vein (antecubital fossa, central vasoconstriction, hypotension, nausea,
line preferred) to prevent extravasa- vomiting, dyspnea. Occasional: Piloerec-
tion. • Use infusion pump to control tion (goose bumps), bradycardia, widen-
flow rate. • Titrate drug to desired ing of QRS complex.
hemodynamic, renal response (optimum
urinary flow determines dosage). ADVERSE EFFECTS/TOXIC
Storage • Do not use solutions darker REACTIONS
than slightly yellow or discolored to yel- High doses may produce ventricular
low, brown, pink to purple (indicates arrhythmias, tachycardia. Pts with occlu-
decomposition of drug). • Stable for sive vascular disease are at high risk for
24 hrs after dilution. further compromise of circulation to
IV INCOMPATIBILITIES extremities, which may result in gangrene.
Tissue necrosis with sloughing may occur
Acyclovir (Zovirax), amphotericin B
with extravasation of IV solution.
complex (Abelcet, AmBisome, Ampho-
tec), cefepime (Maxipime), furosemide NURSING CONSIDERATIONS
(Lasix), insulin, sodium bicarbonate.
BASELINE ASSESSMENT
IV COMPATIBILITIES Pt must be on continuous cardiac moni-
Amiodarone (Cordarone), calcium chlo- toring. Determine weight (for dosage cal-
ride, dexmedetomidine (Precedex), culation). Obtain initial B/P, heart rate,
dilTIAZem (Cardizem), DOBUTamine respirations. Assess patency of IV access.
underlined – top prescribed drug
doravirine/lamivudine/tenofovir 361
INTERVENTION/EVALUATION (Symfi Lo), abacavir/dolutegravir/
Continuously monitor for cardiac arrhyth- lamivudine (Triumeq), abacavir/
mias. Measure urinary output frequently. lamivudine/zidovudine (Trizivir),
If extravasation occurs, immediately infil- bictegravir/emtricitabine/tenofo-
trate affected tissue with 10–15 mL 0.9% vir (Biktarvy), efavirenz/emtric-
NaCl solution containing 5–10 mg phen- itabine/tenofovir (Atripla), or D
tolamine mesylate. Monitor B/P, heart emtricitabine/lopinavir/ritonavir/
rate, respirations q15min during admin- tenofovir (Kaletra).
istration (more often if indicated). Assess
uCLASSIFICATION
cardiac output, pulmonary wedge pres-
sure, or central venous pressure (CVP) PHARMACOTHERAPEUTIC: Nonnucleo-
frequently. Assess peripheral circulation side reverse transcriptase inhibitor,
(palpate pulses, note color/tempera- nucleoside reverse transcriptase
ture of extremities). Immediately notify inhibitor, nucleotide reverse tran-
physician of decreased urinary output, scriptase inhibitor. CLINICAL: Antiret-
cardiac arrhythmias, significant changes roviral agent (anti-HIV).
in B/P, heart rate, or failure to respond
to increase or decrease in infusion rate,
decreased peripheral circulation (cold, USES
pale, mottled extremities). Taper dosage Treatment of HIV-1 infection in adult pts
before discontinuing (abrupt cessation with no antiretroviral treatment history.
of therapy may result in marked hypoten-
sion). Be alert to excessive vasoconstric- PRECAUTIONS
tion (decreased urine output, increased Contraindications: Hypersensitivity to dora-
heart rate, arrhythmias, disproportion- virine, lamivudine, or tenofovir. Concomi-
ate increase in diastolic B/P, decrease in tant use of strong CYP3A inducers (e.g.,
pulse pressure); slow or temporarily stop carBAMazepine, phenytoin, mitotane,
infusion, notify physician. rifAMPin, St. John’s wort), enzalutamide.
Cautions: Hyperlipidemia, psychiatric ill-
ness (e.g., depression, psychosis, suicidal
ideation), renal/hepatic impairment; his-
tory of pathologic fracture, osteoporosis,
doravirine/ osteopenia. Concomitant use of moderate
lamivudine/ CYP3A inducers. Not recommended in pts
with CrCl less than 50 mL/min, end-stage
tenofovir renal disease requiring dialysis.

dor-a-vir-een/la-miv-ue-deen/ten- ACTION
oh-foe-veer Doravirine (nonnucleoside reverse tran-
(Delstrigo) scriptase inhibitor) blocks noncompeti-
j BLACK BOX ALERT j Severe tive HIV-1 reverse transcriptase (does not
exacerbations of hepatitis B virus inhibit DNA polymerases or mitochon-
(HBV) reported in pts co-infected drial DNA polymerase). Lamivudine
with HIV-1 and HBV following (nucleotide reverse transcriptase inhibi-
discontinuation. If discontinuation tor) inhibits HIV reverse transcription via
occurs, monitor hepatic function for
at least several mos. Initiate anti- viral DNA chain termination. Tenofovir
HBV therapy if warranted. (nucleotide reverse transcriptase inhibi-
Do not confuse doravirine/lami- tor) interferes with the HIV RNA-depen-
vudine/tenofovir (Delstrigo) with dent DNA polymerase. Therapeutic
efavirenz/lamivudine/tenofovir Effect: Interferes with HIV-1 replication.

Canadian trade name Non-Crushable Drug High Alert drug


362 doravirine/lamivudine/tenofovir

PHARMACOKINETICS AVAILABILITY (Rx)


Widely distributed. Doravirine metabo- Fixed-Dose Combination Tablets: (dora-
lized in liver. Tenofovir metabolized by virine/lamivudine/tenofovir [TDF]):
enzymatic hydrolysis, mediated by mac- 100 mg/300 mg/300 mg.
rophages and hepatocytes. Protein bind-
D ing: (doravirine): 76%; (lamivudine): ADMINISTRATION/HANDLING
less than 36%, (tenofovir): less than 1%. PO
Peak plasma concentration: (dora- • Give without regard to food.
virine): 2 hrs; (tenofovir): 1 hr. Dora-
virine excreted primarily in urine (6%). INDICATIONS/ROUTES/DOSAGE
Lamivudine excreted primarily in urine HIV Infection
(71%). Tenofovir excreted primarily in PO: ADULTS: 1 tablet once daily.
urine (70%–80%). Half-life: (dora-
virine): 15 hrs; (lamivudine): 5–7 hrs; Dose Modification
(tenofovir): 17 hrs. Concomitant use of rifabutin: Give
additional dose of doravirine 100 mg
LIFESPAN CONSIDERATIONS approx. 12 hrs after fixed-dose combina-
Pregnancy/Lactation: Breastfeed- tion tablet.
ing not recommended due to risk of
Dosage in Renal Impairment
postnatal HIV transmission. Unknown
CrCl greater than 50 mL/min: No dose
if doravirine is secreted in breast milk.
Lamivudine, tenofovir is secreted in adjustment. CrCl less than 50 mL/min,
breast milk. Children: Safety and effi- ESRD requiring HD: Not recommended.
cacy not established. Elderly: Not speci- Dosage in Hepatic Impairment
fied; use caution. Mild to moderate impairment: No
INTERACTIONS dose adjustment. Severe impairment:
Not specified; use caution.
DRUG: NSAIDS (e.g., ibuprofen,
naproxen) may increase nephro- SIDE EFFECTS
toxic effect of tenofovir. Strong CYP3A Occasional (7%–4%): Dizziness, nausea,
inducers (e.g., carBAMazepine, phe- abnormal dreams, insomnia. Rare (3%–
nytoin, rifAMPin), enzalutamide, 2%): Diarrhea, somnolence, rash.
mitotane may decrease concentration/
effect; use contraindicated. Efavirenz, ADVERSE EFFECTS/TOXIC
etravirine, nevirapine may decrease REACTIONS
concentration/effect of doravirine. Hep- May cause new or worsening renal failure
atitis C antivirals (e.g., ledipasvir, including Fanconi syndrome (renal tubular
sofosbuvir) may increase concentra- injury, nonabsorption of essential electro-
tion/effect of tenofovir. Sorbitol may lytes, acids, buffers in renal tubules). Renal
decrease concentration/effect of lami- tubular injury may lead to rhabdomyolysis,
vudine. Doravirine may decrease con- osteomalacia, muscle weakness, myopathy.
centration of ergonovine. HERBAL: St. May decrease bone mineral density, leading
John’s wort may decrease concentra- to pathologic fractures. Fatal lactic acido-
tion/effect; use contraindicated. FOOD: sis, severe hepatomegaly with steatosis
None known. LAB VALUES: May increase (fatty liver) was reported. Fatal cases of
serum alkaline phosphatase, amylase, hepatitis, fulminant hepatitis, hepatic injury
ALT, AST, bilirubin, LDL cholesterol, requiring liver transplantation were re-
GGT, creatine kinase, creatinine, lipase, ported. If therapy is discontinued, pts co-
triglycerides. May decrease serum potas- infected with hepatitis B or C virus have an
sium, phosphate; Hgb, Hct, RBCs. increased risk for viral replication, worsen-

underlined – top prescribed drug


doripenem 363
ing of hepatic function, and may experi- psychiatric symptoms (agitation, delu-
ence hepatic decompensation and/or fail- sions, depression, paranoia, psychosis,
ure. Suicidal ideation, depression, suicide suicidal ideation).
attempt were reported (primarily occurred
PATIENT/FAMILY TEACHING
in pts with prior psychiatric illness). May
induce immune recovery syndrome (in- • Treatment does not cure HIV infection D
flammatory response to dormant opportu- nor reduce risk of transmission. Practice
nistic infections such as Mycobacterium safe sex with barrier methods or
avium, cytomegalovirus, PCP, tuberculosis ­abstinence. • Drug resistance can form
or acceleration of autoimmune disorders if treatment is interrupted; do not run out
including Graves’ disease, polymyositis, of supply. • As immune system strength-
Guillain-Barre). ens, it may respond to dormant infections
hidden within the body. Report any new
NURSING CONSIDERATIONS fever, chills, body aches, cough, night
sweats, shortness of breath. • Fatal
BASELINE ASSESSMENT
cases of liver inflammation or failure have
Obtain LFT, BUN, serum creatinine, CrCl, occurred; report abdominal pain, clay-
eGFR, CD4+ count, viral load, HIV-1 RNA colored stools, yellowing of skin or eyes,
level; urine glucose, urine protein; preg- weight loss. • Report symptoms of kid-
nancy test in female pts of reproductive ney inflammation or disease (decreased
potential. Obtain serum phosphate level in urine output, flank pain, darkened urine);
pts with renal impairment. Test all pts for toxic skin reactions (rash, pustules, skin
HBV infection. Receive full medication eruptions). • Report any psychiatric
history (including herbal products) and symptoms (agitation, delusions, depres-
screen for contraindications/interactions. sion, mood alteration, paranoia, suicidal
Question history of hepatic/renal impair- ideation). • Breastfeeding not recom-
ment, hyperlipidemia, hypersensitivity mended. • Decreased bone density may
reactions, decreased mineral bone den- lead to pathologic fractures; report bone/
sity, osteopenia, psychiatric illness. Offer extremity pain, suspected frac-
emotional support. tures. • Antiretrovirals may cause ex-
INTERVENTION/EVALUATION cess body fat in upper back, neck, breast,
trunk, while also causing decreased body
Monitor CD4+ count, viral load, HIV-1 fat in legs, arms, face. • Do not take
RNA level for treatment effectiveness. newly prescribed medications unless ap-
Monitor LFT; assess for hepatic injury proved by prescriber who originally
(bruising, hematuria, jaundice, right up- started treatment. • Do not take herbal
per abdominal pain, nausea, vomiting, products, esp. St. John’s wort.
weight loss). If discontinuation of drug
regimen occurs, monitor hepatic func-
tion for at least several mos. Initiate anti-
HBV therapy if warranted. Obtain serum doripenem
lactate level if lactic acidosis suspected
(confusion, dyspnea, muscle cramps, dor-i-pen-em
tachypnea). Monitor renal function as Do not confuse Doribax with
clinically indicated. An increase of serum Zovirax, or doripenem with
creatinine greater than 0.4 mg/dL from ertapenem, imipenem, or
baseline may indicate renal impairment. meropenem.
Cough, dyspnea, fever, excess band cells
on CBC may indicate acute infection uCLASSIFICATION
(WBC count may be unreliable in pts with PHARMACOTHERAPEUTIC: Carbap-
uncontrolled HIV infection). Assess skin enem. CLINICAL: Antibiotic.
for toxic skin reactions, rash. Screen for
Canadian trade name Non-Crushable Drug High Alert drug
364 doripenem

USES phosphatase, ALT, AST. May decrease Hgb,


Treatment of complicated intra-abdomi- Hct, platelet count; serum potassium.
nal infections, complicated UTIs (includ-
AVAILABILITY (Rx)
ing pyelonephritis) due to susceptible
gram-positive, gram-negative (including Injection, Powder for Reconstitution: 250
D E. coli, Klebsiella pneumoniae, Proteus mg, 500 mg.
mirabilis, P. aeruginosa), and anaero-
ADMINISTRATION/HANDLING
bic bacteria. OFF-LABEL: Treatment of
intravascular catheter-related blood- IV
stream infection due to ESBL-producing Reconstitution • Reconstitute 250-mg
E. coli and Klebsiella spp. pneumonia, or 500-mg vial with 10 mL Sterile Water
including ventilator-associated. for Injection or 0.9% NaCl. • Shake well
PRECAUTIONS to dissolve. • Further dilute with 100 mL
0.9% NaCl or D5W.
Contraindications: History of serious Rate of administration • Give by
hypersensitivity to doripenem or other intermittent IV infusion (piggyback).
carbapenems (meropenem, imipenem- • Do not give IV push. • Infuse over
cilastatin, ertapenem). Anaphylactic 60 min.
reactions to beta-lactam antibiotics. Storage • Stable for 12 hrs at room
Cautions: Hypersensitivity to penicillins, temperature, 72 hrs if refrigerated when
cephalosporins. Pts with renal impair- diluted in 0.9% NaCl; 4 hrs at room tem-
ment, CNS disorders (e.g., stroke, history perature, 24 hrs if refrigerated when
of seizures). diluted in D5W.
ACTION
IV INCOMPATIBILITIES
Inactivates penicillin-binding proteins,
resulting in inhibition of cell wall syn- DiazePAM (Valium), potassium phos-
thesis. Therapeutic Effect: Produces phate, propofol (Diprivan).
bacterial cell death.
IV COMPATIBILITIES
PHARMACOKINETICS Amiodarone, bumetanide (Bumex),
Penetrates into body fluids, tissues. calcium gluconate, dexamethasone, dil-
Widely distributed. Protein binding: 8%. TIAZem (Cardizem), diphenhydrAMINE
Primarily excreted in urine. Removed by (Benadryl), furosemide (Lasix), heparin,
dialysis. Half-life: 1 hr. hydrocortisone (SOLU-Cortef), HYDRO-
morphone (Dilaudid), insulin, labet-
LIFESPAN CONSIDERATIONS alol (Trandate), LORazepam (Ativan),
P r e g n a n c y / L a c t a t i o n : Distrib- magnesium sulfate, methylPREDNISo-
uted in breast milk. Children: Safety lone (SOLU-Medrol), metoclopramide
and efficacy not established. Elderly: (Reglan), milrinone, morphine, ondan-
Advanced renal insufficiency, end-stage setron (Zofran), pantoprazole (Proto-
renal insufficiency may require dosage nix), potassium chloride.
adjustment.
INDICATIONS/ROUTES/DOSAGE
INTERACTIONS Intra-abdominal Infections
DRUG: Probenecid reduces renal IV: ADULTS, ELDERLY: 500 mg q8h for
excretion of doripenem. May decrease 5–14 days.
valproic acid concentration (do
not use concurrently). HERBAL: None Urinary Tract Infections
significant. FOOD: None known. LAB IV: ADULTS, ELDERLY: 500 mg q8h for
VALUES: May increase serum alkaline 10–14 days.

underlined – top prescribed drug


doxazosin 365
Dosage in Renal Impairment tion at IV injection site. Assess skin for
Creatinine rash. Check mental status; be alert to
Clearance Dosage tremors, possible seizures. Assess sleep
Greater than No adjustment pattern for evidence of insomnia.
50 mL/min
30–50 mL/min 250 mg q8h PATIENT/FAMILY TEACHING D
11–29 mL/min 250 mg q12h • Report tremors, seizures, rash, diar-
Hemodialysis 250 mg q24h; if treating rhea, or other new symptoms.
infection caused by
Pseudomonas aerugi-
nosa: 500 mg q12h on

Continuous
day 1, then 500 g q24h
250 mg q12h
doxazosin
renal
replacement dox-a-zoe-sin
therapy (Apo-Doxazosin , Cardura,
Cardura XL)
Dosage in Hepatic Impairment Do not confuse Cardura with
No dose adjustment. Cardene, Cordarone, Coumadin,
K-Dur, or Ridaura, or doxazo-
SIDE EFFECTS sin with doxapram, doxepin, or
Frequent (10%–6%): Diarrhea, nausea, DOXOrubicin.
headache. Occasional (5%–2%): Altered
mental status, insomnia, rash, abdomi- uCLASSIFICATION
nal pain, constipation, vomiting, edema, PHARMACOTHERAPEUTIC: Alpha-
fever. Rare (less than 2%): Dizziness, adrenergic blocker. CLINICAL: Anti-
cough, oral candidiasis, anxiety, tachy- hypertensive.
cardia, phlebitis at IV site.
ADVERSE EFFECTS/TOXIC USES
REACTIONS Cardura: Treatment of mild to moderate
Antibiotic-associated colitis, other superin- hypertension. Used alone or in combina-
fections (abdominal cramps, severe watery tion with other antihypertensives. Treat-
diarrhea, fever) may occur. Anaphylactic ment of urinary outflow obstruction and/or
reactions in pts receiving beta-lactams obstruction and irritation associated with
have occurred. Seizures may occur in benign prostatic hyperplasia (BPH). Car-
those with CNS disorders (brain lesions, dura XL: Treatment of urinary outflow
history of seizures) or with bacterial men- obstruction and/or obstruction and irrita-
ingitis or severe impaired renal function. tion associated with benign prostatic hyper-
plasia. OFF-LABEL: Pediatric hypertension.
NURSING CONSIDERATIONS Facilitate distal ureteral stone expulsion.
BASELINE ASSESSMENT Erectile dysfunction in pts with BPH.
Question pt for history of allergies, particu- PRECAUTIONS
larly to beta-lactams, penicillins, cephalo-
sporins. Inquire about history of seizures. Contraindications: Hypersensitivity to
doxazosin or other quinazolines (prazo-
INTERVENTION/EVALUATION sin, terazosin). Cautions: Constipation,
Monitor for signs of hypersensitivity reac- ileus, GI obstruction, hepatic impairment.
tion during first dose. Monitor daily pat-
tern of bowel activity, stool consistency. ACTION
Monitor for nausea, vomiting. Evaluate Hypertension: Selectively blocks
hydration status. Evaluate for inflamma- alpha1-adrenergic receptors, decreasing

Canadian trade name Non-Crushable Drug High Alert drug


366 doxazosin
peripheral vascular resistance. BPH: extended-release tablets given with
Inhibits postsynaptic alpha-adrenergic morning meal.
receptors in prostatic stromal and
bladder neck tissues. Therapeutic INDICATIONS/ROUTES/
Effect: Hypertension: Causes peripheral DOSAGE
D vasodilation, lowering B/P. BPH: Relaxes Hypertension
smooth muscle of bladder, prostate, reduc- PO: (Immediate-Release): ADULTS,
ing BPH symptoms. ELDERLY: Initially, 1 mg once daily. May
be increased to 2 mg once daily. There-
PHARMACOKINETICS after, may increase upward over several
Route Onset Peak Duration wks to a maximum of 16 mg/day.
PO (antihy- 1–2 hrs 2–6 hrs 24 hrs
Benign Prostatic Hyperplasia
pertensive)
PO: (Immediate-Release): ADULTS,
Well absorbed from GI tract. Protein ELDERLY: Initially, 1 mg/day. May
binding: 98%–99%. Metabolized in titrate at intervals of 1–2 wks by
liver. Primarily eliminated in feces. doubling daily dose to 2 mg, 4 mg,
Not removed by hemodialysis. Half- and 8 mg. Maximum: 8 mg/day.
life: 19–22 hrs. (Extended-Release): Initially, 4 mg/
day. May increase to 8 mg in 3–4 wks.
LIFESPAN CONSIDERATIONS Note: When switching to extended-
Pregnancy/Lactation: Unknown if release, omit evening dose prior to
drug crosses placenta or is distributed starting morning dose.
in breast milk. Children: Safety and
Dosage in Renal Impairment
efficacy not established. Elderly: May
be more sensitive to hypotensive effects. No dose adjustment.
Dosage in Hepatic Impairment
INTERACTIONS
Mild to moderate impairment: Use
DRUG: Strong CYP3A4 inducers (e.g., caution. Severe Impairment: Avoid
carBAMazepine, phenytoin, rifAMPin) use.
may decrease concentration/effect. Strong
CYP3A4 inhibitors (e.g., clarithro- SIDE EFFECTS
mycin, ketoconazole, ritonavir) may Frequent (20%–10%): Dizziness, asthe-
increase concentration/effect. HERBAL: nia, headache, edema. Occasional
St. John’s wort may decrease concentra- (9%–3%): Nausea, pharyngitis, rhinitis,
tion/effect. Yohimbe may decrease antihy- pain in extremities, drowsiness. Rare
pertensive effect. FOOD: None known. LAB (2%–1%): Palpitations, diarrhea, consti-
VALUES: None significant. pation, dyspnea, myalgia, altered vision,
anxiety.
AVAILABILITY (Rx)
Tablets: 1 mg, 2 mg, 4 mg, 8 mg. ADVERSE EFFECTS/TOXIC
Tablets, Extended-Release: 4 mg, 8 REACTIONS
mg. First-dose syncope (hypotension with
sudden loss of consciousness) may
ADMINISTRATION/HANDLING occur 30–90 min after initial dose of 2
PO mg or greater, too-rapid increase in dos-
• Give without regard to food. • Do age, addition of another antihypertensive
not break, crush, dissolve, or divide agent to therapy. First-dose syncope may
extended-release tablet. • Immediate- be preceded by tachycardia (pulse rate
release tablets given morning or evening; 120–160 beats/min).

underlined – top prescribed drug


doxepin 367

NURSING CONSIDERATIONS in pts with difficulty staying asleep. Topi-


cal: Treatment of pruritus associated with
BASELINE ASSESSMENT atopic dermatitis. OFF-LABEL: Treatment
Give first dose at bedtime. If initial dose of neurogenic pain, treatment of anxiety.
is given during daytime, pt must remain
recumbent for 3–4 hrs. Assess B/P, pulse PRECAUTIONS D
immediately before each dose and q15– Contraindications: Hypersensitivity to dox­
30 min until B/P is stabilized (be alert to epin. Glaucoma, hypersensitivity to other
fluctuations). tricyclic antidepressants, urinary reten-
tion, use of MAOIs within 14 days. Cau-
INTERVENTION/EVALUATION tions: Cardiac/hepatic/renal disease, pts
Monitor B/P, I&O. Monitor pulse dili- at risk for suicidal ideation, respiratory
gently (first-dose syncope may be pre- compromise, sleep apnea, history of bowel
ceded by tachycardia). Assess for edema, obstruction, increased IOP, glaucoma, his-
headache. Assist with ambulation if dizzi- tory of seizures, history of urinary retention/
ness, light-headedness occurs. obstruction, hyperthyroidism, prostatic
PATIENT/FAMILY TEACHING
hypertrophy, hiatal hernia, elderly.
• Full therapeutic effect may not occur ACTION
for 3–4 wks. • May cause syncope Increases synaptic concentrations of
(fainting); go from lying to standing norepinephrine, serotonin by inhibit-
slowly. • Avoid tasks that require alert- ing reuptake. Therapeutic Effect:
ness, motor skills until response to drug Produces antidepressant, anxiolytic
is established. effects.
PHARMACOKINETICS
PO: Rapidly absorbed from GI tract.
doxepin Protein binding: 80%–85%. Metabo-
lized in liver. Primarily excreted in
dox-e-pin urine. Not removed by hemodialysis.
(Silenor, Sinequan , Zonalon) Half-life: 6–8 hrs. Topical: Absorbed
j BLACK BOX ALERT jIncreased through skin. Distributed to body tis-
risk of suicidal ideation and behav- sues. Metabolized to active metabolite.
ior in children, adolescents, young Excreted in urine.
adults 18–24 yrs with major depres-
sive disorder, other psychiatric
disorders. LIFESPAN CONSIDERATIONS
Do not confuse doxepin with Pregnancy/Lactation: Crosses placenta.
digoxin, doxapram, doxazosin, Distributed in breast milk. Chil-
Doxidan, or doxycycline, or dren: Safety and efficacy not estab-
SINEquan with SEROquel, or lished in pts younger than 12 yrs.
Singulair. Elderly: Increased risk of toxicity
(lower dosages recommended). Avoid
uCLASSIFICATION doses greater than 6 mg/day due to anti-
PHARMACOTHERAPEUTIC: Tricyclic. cholinergic effects, sedation, and ortho-
CLINICAL: Antidepressant, antianxi- static hypotension.
ety, antineuralgic, antipruritic.
INTERACTIONS
DRUG: Alcohol, other CNS depres-
USES sants (e.g., lorazepam, morphine,
Treatment of depression and/or anxiety. zolpidem) may increase CNS, respi-
Silenor (only): Treatment of insomnia ratory depression. MAOIs (e.g.,

Canadian trade name Non-Crushable Drug High Alert drug


368 doxepin
phenelzine, selegiline) may increase 10–25 mg at bedtime. May increase by
risk of seizures, hyperpyrexia, hyperten- 10–25 mg/day every 3–7 days.
sive crisis (discontinue at least 2 wks
prior to starting doxepin). Anticho- Insomnia (Silenor only)
linergic agents (e.g., aclidinium, PO: ADULTS: 3–6 mg (give within 30
D ipratropium, umeclidinium) may min of bedtime).  ELDERLY: 3 mg (give
increase anticholinergic effect. May within 30 min of bedtime). May increase
increase QT interval-prolonging effect of to 6 mg once daily.
dronedarone. Strong CYP2D6 inhib-
Pruritus Associated with Atopic
itors (e.g., buPROPion, PARoxetine)
Dermatitis
may increase concentration/effect.
Topical: ADULTS, ELDERLY: Apply thin
HERBAL: Herbals with sedative prop-
erties (e.g., chamomile, kava kava, film 4 times/day at 3- to 4-hr intervals.
valerian) may increase CNS depression. Not recommended for more than 8 days.
St. John’s wort may decrease concen- Dosage in Renal Impairment
tration/effects. FOOD: None known. LAB No dose adjustment.
VALUES: May alter serum glucose, ECG
readings. Therapeutic serum level: Dosage in Hepatic Impairment
110–250 ng/mL; toxic serum level: Use lower initial dose; adjust gradually.
greater than 300 ng/mL. Silenor: Initially, 3 mg once daily.

AVAILABILITY (Rx) SIDE EFFECTS


Capsules: 10 mg, 25 mg, 50 mg, 75 mg, Frequent: PO: Orthostatic hypotension,
100 mg, 150 mg. Cream: (Prudoxin, Zona- drowsiness, dry mouth, headache,
lon): 5%. Oral Concentrate: 10 mg/mL. increased appetite, weight gain, nausea,
Tablets: (Silenor): 3 mg, 6 mg. unusual fatigue, unpleasant taste. Topi-
cal: Edema, increased pruritus, eczema,
ADMINISTRATION/HANDLING burning, tingling, stinging at application
PO site, altered taste, dizziness, drowsiness,
• Give with food, milk if GI distress dry skin, dry mouth, fatigue, headache,
occurs. • Dilute concentrate in 4-oz thirst. Occasional: PO: Blurred vision,
glass of water, milk, or orange, tomato, confusion, constipation, hallucinations,
prune, pineapple juice. Incompatible difficult urination, eye pain, irregular
with carbonated drinks. • Give larger heartbeat, fine muscle tremors, nervous-
portion of daily dose at bedtime. ness, impaired sexual function, diarrhea,
diaphoresis, heartburn, insomnia. Sile-
Topical nor: Nausea, upper respiratory infection.
• Apply thin film of cream on affected Topical: Anxiety, skin irritation/cracking,
areas of skin. • Do not use for more than nausea. Rare: PO: Allergic reaction, alo-
8 days. • Do not use occlusive dressing. pecia, tinnitus, breast enlargement. Topi-
INDICATIONS/ROUTES/DOSAGE cal: Fever, photosensitivity.
Depression, Anxiety ADVERSE EFFECTS/TOXIC
Note: Gradually taper dose upon dis- REACTIONS
continuation of antidepressant therapy. Abrupt or too-rapid withdrawal may
PO: ADULTS: Initially, 25–50 mg/day at result in headache, malaise, nausea,
bedtime or in 2–3 divided doses. May vomiting, vivid dreams. Overdose may
increase gradually to usual dose of 100 produce confusion, severe drowsiness,
mg–300 mg/day (single dose should agitation, tachycardia, arrhythmias,
not exceed 150 mg). ELDERLY: Initially, shortness of breath, vomiting.

underlined – top prescribed drug


DOXOrubicin 369
tion may be life threatening. Severe
NURSING CONSIDERATIONS myelosuppression may occur.
BASELINE ASSESSMENT Must be administered by personnel
trained in administration/handling
Assess B/P, pulse, ECG (those with history of chemotherapeutic agents.
of cardiovascular disease). Perform CBC, Secondary acute myelogenous
serum electrolyte tests before long-term leukemia and myelodysplastic syn- D
therapy. Assess pt’s appearance, behavior, drome have been reported. Potent
vesicant.
level of interest, mood, suicidal ideation, Do not confuse DOXOrubicin
sleep pattern. with dactinomycin, DAUNOru-
INTERVENTION/EVALUATION bicin, doxazosin, epiRUBicin,
Monitor B/P, pulse, weight. Perform CBC, IDArubicin, or valrubicin, or
serum electrolyte tests periodically to Adriamycin with Aredia or
assess renal/hepatic function. Monitor idamycin.
mental status, suicidal ideation. Supervise uCLASSIFICATION
suicidal-risk pt closely during early ther-
apy (as depression lessens, energy level PHARMACOTHERAPEUTIC: Anthra-
improves, increasing suicide potential). cycline, topoisomerase II inhibitor.
Assess appearance, behavior, speech pat- CLINICAL: Antineoplastic.
tern, level of interest, mood. Therapeu-
tic serum level: 110–250 ng/mL; toxic USES
serum level: greater than 300 ng/mL.
Adriamycin: Treatment of acute lym-
PATIENT/FAMILY TEACHING phocytic leukemia (ALL), acute myeloid
• Do not discontinue abruptly. • Change leukemia (AML), Hodgkin’s lymphoma,
positions slowly to avoid dizzi- malignant lymphoma; breast, gastric,
ness. • Avoid tasks that require alertness, small-cell lung, ovarian, epithelial, thy-
motor skills until response to drug is estab- roid, bladder carcinomas; neuroblas-
lished. • Do not cover affected area with toma, Wilms tumor, osteosarcoma, soft
occlusive dressing after applying tissue sarcoma. Doxil, Lipodox: Treat-
cream. • May cause dry mouth. • Avoid ment of AIDS-related Kaposi’s sarcoma,
alcohol, limit caffeine. • May increase advanced ovarian cancer. Used with
appetite. • Avoid exposure to sunlight/ bortezomib to treat multiple myeloma
artificial light source. • Therapeutic ef- in pts who have not previously received
fect may be noted within 2–5 days, maxi- bortezomib and have received at least one
mum effect within 2–3 wks. • Report previous treatment. OFF-LABEL: Adria-
worsening depression, suicidal ideation, mycin: Multiple myeloma, endometrial
unusual changes in behavior (esp. at initia- carcinoma, uterine sarcoma; head and
tion of therapy or with changes in dosage). neck cancer, liver, kidney cancer. Doxil:
Metastatic breast cancer, Hodgkin’s lym-
phoma, cutaneous T-cell lymphomas,
advanced soft tissue sarcomas, recurrent
DOXOrubicin or metastatic cervical cancer, advanced
or metastatic uterine sarcoma.
dox-o-rue-bi-sin
(Adriamycin, Caelyx , Doxil, PRECAUTIONS
Lipodox-50) Contraindications: Hypersensitivity to
j BLACK BOX ALERT j May DOXOrubicin. Adriamycin: Severe
cause concurrent or cumulative hepatic impairment, severe myocar-
myocardial toxicity. Acute allergic dial insufficiency, recent MI (within
or anaphylaxis-like infusion reac-

Canadian trade name Non-Crushable Drug High Alert drug


370 DOXOrubicin
4–6 wks), severe arrhythmias. Previ- John’s wort may decrease concentration.
ous or concomitant treatment with high Echinacea may decrease therapeutic effect.
accumulative doses of DOXOrubicin, FOOD: None known. LAB VALUES: May
DAUNOrubicin, IDArubicin, or other cause ECG changes, increase serum uric
anthracyclines or anthracenediones; acid. May reduce neutrophil, RBC counts.
D severe, persistent drug-induced myelo-
suppression or baseline ANC count less AVAILABILITY (Rx)
than 1,500 cells/mm3. Doxil: Breast- Injection, Powder for Reconstitution: 10
feeding (Canada). Cautions: Hepatic mg, 20 mg, 50 mg. Injection Solution:
impairment. Cardiomyopathy, preexisting (Adriamycin): 2 mg/mL (5-mL, 10-mL,
myelosuppression, severe HF. Pts who 25-mL, 100-mL vial). Lipid Complex:
received radiation therapy. (Doxil, Lipodox-50): 2 mg/mL (10 mL,
25 mL).
ACTION
Inhibits DNA, RNA synthesis by binding ADMINISTRATION/HANDLING
with DNA strands. Liposomal encapsula- b ALERT c Wear gloves. If powder or
tion increases uptake by tumors, prolongs solution comes into contact with skin,
drug action, may decrease toxicity. Thera- wash thoroughly. Avoid small veins; swol-
peutic Effect: Prevents cell division. len/edematous extremities; areas overly-
ing joints, tendons. • (Doxil): Do not use
PHARMACOKINETICS with in-line filter or mix with any diluent
Widely distributed. Protein binding: except D5W. May be carcinogenic, muta-
74%–76%. Does not cross blood-brain genic, teratogenic. Handle with extreme
barrier. Metabolized in liver. Primarily care during preparation/administration.
eliminated by biliary system. Not removed
by hemodialysis. Half-life: 20–48 hrs.
IV
LIFESPAN CONSIDERATIONS Reconstitution • Reconstitute vials of
Pregnancy/Lactation: If possible, powder with 0.9% NaCl to provide con-
avoid use during pregnancy, esp. first tri- centration of 2 mg/mL. • Shake vial;
mester. Breastfeeding not recommended. allow contents to dissolve. • Withdraw
Children/Elderly: Cardiotoxicity may appropriate volume of air from vial dur-
be more frequent in pts younger than 2 ing reconstitution (avoids excessive pres-
yrs or older than 70 yrs. sure buildup). • May be further diluted
INTERACTIONS with 50–1,000 mL D5W or 0.9% NaCl
and given as continuous infu-
DRUG: CycloSPORINE may increase sion. • (Doxil): Dilute each dose in
concentration/effect; risk of hematologic 250 mL D5W (doses greater than 90 mg
toxicity. Bevacizumab, DAUNOrubicin in 500 mL D5W).
may increase risk of cardiotoxicity. Bone Rate of administration • (Adriamy-
marrow depressants (e.g., cladrib- cin): For IV push, administer into tubing of
ine) may increase myelosuppression. freely running IV infusion of D5W or 0.9%
Strong CYP3A4 inducers (e.g., carBA- NaCl, preferably via butterfly needle over
Mazepine, phenytoin, rifAMPin) may 3–5 min (avoids local erythematous streak-
decrease concentration/effect. Strong ing along vein and facial flushing). • Must
CYP3A4 inhibitors (e.g., clarithro- test for flashback q30sec to be certain
mycin, ketoconazole, ritonavir) may needle remains in vein during injection. IV
increase concentration/effect. Live virus piggyback over 15–60 min or continuous
vaccines may potentiate virus replication, infusion. • Extravasation produces imme-
increase vaccine side effects, decrease pt’s diate pain, severe local tissue damage. Ter-
antibody response to vaccine. HERBAL: St. minate administration immediately;
underlined – top prescribed drug
DOXOrubicin 371
withdraw as much medication as possible, Kaposi’s Sarcoma
obtain extravasation kit, follow protocol. IV: (Doxil, Lipodox): ADULTS: 20 mg/
• (Doxil): Give as infusion over 60 min. m2 q3wks infused over 30 min. Continue
Do not use in-line filter. until disease progression or unaccept-
Storage • (Adriamycin powder): able toxicity.
Store at room temperature. • Reconsti- D
tuted vials stable for 7 days at room Ovarian Cancer
temperature, 15 days if refrigerated. IV: (Doxil, Lipodox): ADULTS: 50 mg/
Infusions stable for 48 hrs at room tem- m2 q4wks. Continue until disease pro-
perature. • Protect from prolonged gression or unacceptable toxicity.
exposure to sunlight; discard unused Multiple Myeloma
solution. • (Adriamycin solution): IV: (Doxil, Lipodox): ADULTS: 30 mg/
Refrigerate vials. Solutions diluted in m2/dose on day 4 q3wks (in combination
D5W or 0.9% NaCl stable for 48 hrs at with bortezomib). Continue until disease
room temperature. • (Doxil): Refrig- progression or unacceptable toxicity.
erate unopened vials. After solution is
diluted, use within 24 hrs. Dosage in Renal Impairment
No dose adjustment.
IV INCOMPATIBILITIES
DOXOrubicin: Allopurinol (Aloprim), Dose Modifications
amphotericin B complex (Abelcet, AmBi- Adriamycin
some, Amphotec), cefepime (Maxipime), Neutropenic fever/Infection: Reduce
furosemide (Lasix), ganciclovir (Cyto- dose to 75%. ANC less than 1,000
vene), heparin, piperacillin/tazobactam cells/mm3: Delay treatment until ANC
(Zosyn), propofol (Diprivan). Doxil: Do 1,000 cells/mm3 or more. Platelets less
not mix with any other medications. than 100,000/mm3: Delay treatment
until platelets 100,000 cells/mm3 or more.
IV COMPATIBILITIES Doxil
Dexamethasone (Decadron), diphen- Adjustments for hand-foot syn-
hydrAMINE (Benadryl), granisetron drome, stomatitis, hematologic
(Kytril), HYDROmorphone (Dilaudid), toxicities: Refer to manufacturer’s
LORazepam (Ativan), morphine, ondan- guidelines.
setron (Zofran).
Dosage in Hepatic Impairment
INDICATIONS/ROUTES/DOSAGE
ADRIAMYCIN
b ALERT c Refer to individual proto-
cols. Hepatic Function Dosage
ALT, AST 2–3 times 75% of normal
Usual Dosage ULN dose
IV: (Adriamycin): ADULTS: (Single-agent ALT, AST greater than 3 50% of normal
therapy): 60–75 mg/m2 as a single dose times ULN or bilirubin dose
1.2–3 mg/dL
every 21 days, 20 mg/m2 once wkly. (Com- Bilirubin 3.1–5 mg/dL 25% of normal
bination therapy): 40–75 mg/m2 q21– dose
28 days. Because of risk of cardiotoxicity, Bilirubin greater than 5 Not recom-
do not exceed cumulative dose of 550 mg/ mg/dL mended
m2 (400–450 mg/m2 for those previously ULN = upper limit of normal.
treated with related compounds or irradia-
tion of cardiac region). CHILDREN: (Sin- DOXIL
gle-agent therapy): 60–75 mg/ Hepatic Function Dosage
m2 q3wks. (Combination therapy): 40– Bilirubin 1.2–3 mg/ 50% of normal dose
75 mg/m2 q21–28 days. dL

Canadian trade name Non-Crushable Drug High Alert drug


372 doxycycline
Hepatic Function Dosage PATIENT/FAMILY TEACHING
Bilirubin greater 25% of normal dose • Hair loss is reversible, but new hair
than 3 mg/dL growth may have different color, texture.
New hair growth resumes 2–3 mos after
SIDE EFFECTS last therapy dose. • Maintain strict oral
D hygiene. • Do not have immunizations
Frequent: Complete alopecia (scalp,
axillary, pubic hair), nausea, vomit- without physician’s approval (drug lowers
ing, stomatitis, esophagitis (esp. if drug resistance). • Avoid contact with those
is given on several successive days), who have recently received live virus vac-
reddish urine. Doxil: Nausea. Occa- cine. • Promptly report fever, sore
sional: Anorexia, diarrhea; hyper- throat, signs of local infection, unusual
pigmentation of nailbeds, phalangeal, bruising/bleeding from any site. • Report
dermal creases. Rare: Fever, chills, con- persistent nausea/vomiting. • Avoid alco-
junctivitis, lacrimation. hol (may cause GI irritation, a common
side effect with liposomal DOXOrubicin).
ADVERSE EFFECTS/
TOXIC REACTIONS
Myelosuppression manifested as hema-
tologic toxicity (principally leukopenia doxycycline
and, to lesser extent, anemia, thrombocy-
topenia) generally occurs within 10–15 dox-i-sye-kleen
days, returns to normal levels by third (Acticlate, Adoxa, Apo-Doxy ,
wk. Cardiotoxicity (either acute, mani- Avidoxy, Doryx, Doxy-100, Oracea,
fested as transient ECG abnormalities, or Vibramycin)
chronic, manifested as HF) may occur. Do not confuse doxycycline
with dicyclomine or doxepin,
NURSING CONSIDERATIONS Monodox with Maalox, Oracea
with Orencia, Vibramycin with
BASELINE ASSESSMENT Vancomycin or Vibativ, or Vibra-
Obtain ANC, CBC, erythrocyte counts Tabs with Vibativ.
before and at frequent intervals during
therapy. Obtain ECG before therapy, LFT uCLASSIFICATION
before each dose. Antiemetics may be PHARMACOTHERAPEUTIC: Tetracy-
effective in preventing, treating nausea. cline. CLINICAL: Antibiotic.
Offer emotional support.
INTERVENTION/EVALUATION USES
Monitor for stomatitis (burning or erythema Treatment of susceptible infections due to
of oral mucosa at inner margin of lips, dif- H. ducreyi, Pasteurella pestis, P. tular-
ficulty swallowing). Observe IV injection site ensis, Bacteroides spp., V. cholerae,
for infiltration, vein irritation. May lead to Brucella spp., Rickettsiae, Y. pestis,
ulceration of mucous membranes within Francisella tularensis, M. pneumoniae,
2–3 days. Assess dermal creases, nailbeds including brucellosis, chlamydia, chol-
for hyperpigmentation. Monitor hemato- era, granuloma inguinale, lymphogranu-
logic status, renal/hepatic function studies, loma venereum, malaria prophylaxis,
serum uric acid levels. Monitor daily pattern nongonococcal urethritis, pelvic inflam-
of bowel activity, stool consistency. Monitor matory disease (PID), plague, psittaco-
for hematologic toxicity (fever, sore throat, sis, relapsing fever, rickettsia infections,
signs of local infection, unusual bruising/ primary and secondary syphilis, tula-
bleeding from any site), symptoms of ane- remia. (Oracea): Treatment of inflam-
mia (excessive fatigue, weakness). matory lesions in adults with rosacea.
underlined – top prescribed drug
doxycycline 373
OFF-LABEL: Sclerosing agent for pleural Reconstitution: 100 mg. Oral Suspen-
effusion; vancomycin-resistant entero- sion: 25 mg/5 mL. Syrup: 50 mg/5 mL.
cocci (VRE); alternative for MRSA, treat- Tablets: 20 mg, 50 mg, 75 mg, 100 mg,
ment of refractory periodontitis, juvenile 150 mg.
periodontitis. Tablets, Delayed-Release: 50 mg,
75 mg, 100 mg, 150 mg, 200 mg. D
PRECAUTIONS
Contraindications: Hypersensitivity to dox- ADMINISTRATION/HANDLING
ycycline, other tetracyclines. Cautions: His- b ALERT c Do not administer IM or SQ.
tory or predisposition to oral candidiasis Space doses evenly around clock.
(Oracea). Avoid use during pregnancy, dur-
ing tooth development in children. Avoid IV
prolonged exposure to sunlight. Reconstitution • Reconstitute each
100-mg vial with 10 mL Sterile Water for
ACTION Injection for concentration of 10 mg/
Inhibits bacterial protein synthesis by mL. • Further dilute each 100 mg with
binding to ribosomes. May cause altera- at least 100 mL D5W, 0.9% NaCl, lactated
tions in the cytoplasmic membrane. Ringer’s.
Therapeutic Effect: Bacteriostatic. Rate of administration • Give by
intermittent IV infusion (piggyback). •
PHARMACOKINETICS Infuse over 1–4 hrs.
Rapidly absorbed after PO administra- Storage • After reconstitution, IV infu-
tion. Protein binding: 90%. Partially sion (piggyback) is stable for 12 hrs at
excreted in urine; partially eliminated in room temperature or 72 hrs if refriger-
bile. Half-life: 15–24 hrs. ated. • Protect from direct sunlight.
Discard if precipitate forms.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses pla- PO
centa; distributed in breast milk. Chil- • Oral suspension is stable for 2 wks at
dren: May cause permanent discoloration room temperature. • Give with full
of teeth, enamel hypoplasia. Elderly: No glass of fluid. • Instruct pt to sit up for
age-related precautions noted. 30 min after taking to reduce risk of
esophageal irritation and ulcer-
INTERACTIONS ation. • Give without regard to food.
DRUG: Antacids containing alumi- Oracea should be given 1 hr before or 2
num, calcium, magnesium; laxatives hrs after meals. • Avoid concurrent use
containing magnesium, oral iron of antacids, milk; separate by 2 hrs.
preparations decrease absorption. IV INCOMPATIBILITIES
Barbiturates, carBAMazepine may
decrease concentration/effect. Chole- Allopurinol (Aloprim), heparin, piper-
styramine may decrease absorption. acillin/tazobactam (Zosyn).
HERBAL: None significant. FOOD: None
IV COMPATIBILITIES
known. LAB VALUES: May increase
serum alkaline phosphatase, amylase, Acyclovir (Zovirax), amiodarone (Corda-
bilirubin, ALT, AST. May alter CBC. rone), dexmedetomidine (Precedex), dil-
TIAZem (Cardizem), granisetron (Kytril),
AVAILABILITY (Rx) HYDROmorphone (Dilaudid), magne-
40 mg, 50 mg, 75 mg, 100
Capsules:
sium sulfate, meperidine (Demerol),
mg, 150 mg. Injection, Powder for morphine, ondansetron (Zofran), propo-
fol (Diprivan).

Canadian trade name Non-Crushable Drug High Alert drug


374 dronabinol

INDICATIONS/ROUTES/DOSAGE
Usual Dosage
dronabinol
PO: ADULTS, ELDERLY, CHILDREN OLDER
droe-nab-i-nol
THAN 8 YRS, WEIGHING MORE THAN 45
(Marinol, Syndros)
KG: 100–200 mg/day in 1–2 divided
D Do not confuse dronabinol with
doses. IV: 100 mg q12h. IV/PO: CHILDREN
droperidol.
OLDER THAN 8 YRS, WEIGHING 45 KG OR
LESS: 2–4 mg/kg/day (Maximum: 200 uCLASSIFICATION
mg/day) in 1–2 divided doses.
PHARMACOTHERAPEUTIC: Cannabi-
Dosage in Renal/Hepatic Impairment noid (Schedule III). CLINICAL: An-
No dose adjustment. tinausea, antiemetic, appetite stimu-
lant.
SIDE EFFECTS
Frequent: Anorexia, nausea, vomiting,
diarrhea, dysphagia, photosensitivity (may USES
be severe). Occasional: Rash, urticaria. Prevention, treatment of nausea/vom-
iting due to cancer chemotherapy in
ADVERSE EFFECTS/TOXIC pts who failed to respond to con-
REACTIONS ventional treatment. Treatment of
Superinfection (esp. fungal), benign anorexia associated with weight loss
intracranial hypertension (headache, in pts with AIDS. OFF-LABEL: Cancer-
visual changes) may occur. Hepatotoxic- related anorexia.
ity, fatty degeneration of liver, pancreatitis
occur rarely. PRECAUTIONS
Contraindications: Hypersensitivity to
NURSING CONSIDERATIONS dronabinol, sesame oil (capsule), alco-
BASELINE ASSESSMENT
hol (oral solution), marijuana; receiving
or recently received disulfiram- or met-
Question for history of allergies, esp. to ronidazole-containing products within
tetracyclines, sulfites. 14 days (oral solution). Cautions: His-
INTERVENTION/EVALUATION tory of psychiatric illness, schizophre-
Monitor daily pattern of bowel activity, nia, history of substance abuse, mania,
stool consistency. Assess skin for rash. depression, seizure disorder, hepatic
Monitor LOC due to potential for in- impairment, elderly.
creased intracranial pressure (ICP). Be ACTION
alert for superinfection: fever, vomiting,
diarrhea, anal/genital pruritus, oral muco- Exact mechanism unknown. May inhibit
sal changes (ulceration, pain, erythema). endorphins in brain’s emetic center, sup-
press prostaglandins synthesis or effect
PATIENT/FAMILY TEACHING on cannabinoid receptor in CNS. Thera-
• Avoid unnecessary exposure to sun- peutic Effect: Inhibits nausea/vomit-
light. • Do not take with antacids, iron ing, stimulates appetite.
products. • Complete full course of
therapy. • After application of dental PHARMACOKINETICS
gel, avoid brushing teeth, flossing the Well absorbed after PO administration,
treated areas for 7 days. • Report se- only 10%–20% reaches systemic circu-
vere diarrhea. • May cause nausea, lation. Protein binding: 97%. Undergoes
vomiting. If GI upset occurs, may take first-pass metabolism. Highly lipid sol-
with small amount food; however, Oracea uble. Primarily excreted in feces. Half-
should be taken on an empty stomach. life: 25–36 hrs.

underlined – top prescribed drug


dronabinol 375

LIFESPAN CONSIDERATIONS (Syndros): Initially, 2.1 mg twice daily.


Pregnancy/Lactation: Unknown if drug May gradually increase dose in 2.1-mg
crosses placenta. Distributed in breast increments. Maximum: 8.4 mg twice
milk. Children: Not recommended. daily.
Elderly: Monitor carefully during therapy. Dosage in Renal/Hepatic Impairment D
INTERACTIONS No dose adjustment.
DRUG: Alcohol, other CNS sup- SIDE EFFECTS
pressants (e.g., LORazepam, mor- Frequent (24%–3%): Euphoria, dizziness,
phine, zolpidem) may increase CNS paranoid reaction, drowsiness. Occa-
depression. Sympathomimetics may sional (less than 3%–1%): Asthenia, ataxia,
increase risk of hypertension, tachycar- confusion, abnormal thinking, deperson-
dia. Anticholinergics (e.g., glycopyr- alization. Rare (less than 1%): Diarrhea,
rolate, scopolamine) may increase depression, nightmares, speech difficulties,
drowsiness, tachycardia. HERBAL: None headache, anxiety, tinnitus, flushed skin.
significant. FOOD: None known. LAB
VALUES: None significant. ADVERSE EFFECTS/TOXIC
REACTIONS
AVAILABILITY (Rx)
Mild intoxication may produce increased
Capsules: (Gelatin [Marinol]): 2.5 mg, 5 sensory awareness (taste, smell, sound),
mg, 10 mg. Oral Solution: (Syndros): 5 altered time perception, reddened con-
mg/mL. junctiva, dry mouth, tachycardia. Mod-
ADMINISTRATION/HANDLING erate intoxication may produce memory
impairment, urinary retention. Severe
PO intoxication may produce lethargy,
• Store in cool environment. May refriger- decreased motor coordination, slurred
ate capsules. • May administer without speech, orthostatic hypotension.
regard to food. Give before meals if used for
appetite stimulant. • Oral solution: NURSING CONSIDERATIONS
Always use enclosed calibrated syringe.
Take each dose with a full glass of water. BASELINE ASSESSMENT
Assess dehydration status if excessive
INDICATIONS/ROUTES/DOSAGE vomiting occurs (skin turgor, mucous
Prevention of Chemotherapy-Induced membranes, urinary output).
Nausea and Vomiting
INTERVENTION/EVALUATION
PO: ADULTS, ELDERLY, CHILDREN: (Mari-
nol): Initially, 5 mg/m2 1–3 hrs before Supervise closely for serious mood, behav-
chemotherapy, then q2–4h after chemo- ioral responses, esp. in pts with history of
therapy for total of 4–6 doses/day. May psychiatric illness. Monitor B/P, heart rate.
increase by 2.5 mg/m2 up to 15 mg/m2 per PATIENT/FAMILY TEACHING
dose. (Syndros): Initially, 2.1–4.2 mg/
• Change positions slowly to avoid dizzi-
m2 1–2 hrs prior to chemotherapy, then
ness. • Relief from nausea/vomiting
q2–4 hrs after chemotherapy for total of
generally occurs within 15 min of drug
4–6 doses/day. May increase in incre-
administration. • Do not take any other
ments of 2.1 mg/m2. Maximum: 12.6
medications, including OTC, without phy-
mg/m2/dose and 4 to 6 doses per day.
sician approval. • Avoid alcohol, barbi-
Appetite Stimulant turates. • Avoid tasks that require alert-
PO: ADULTS, ELDERLY: (Marinol): Ini- ness, motor skills until response to drug
tially, 2.5 mg twice daily (before lunch is established. • For appetite stimula-
and dinner). Range: 2.5–20 mg/day. tion, take before lunch and dinner.

Canadian trade name Non-Crushable Drug High Alert drug


376 dulaglutide

LIFESPAN CONSIDERATIONS
dulaglutide Pregnancy/Lactation: Unknown if
doo-la-gloo-tide di­
stributed in breast milk. Must either
(Trulicity) discontinue drug or discontinue breast-
feeding. Children: Safety and efficacy not
D j BLACK BOX ALERT jContrain-
dicated in pts with a personal/ established. Elderly: No age-related pre-
family history of medullary thyroid cautions noted.
carcinoma (MTC) or in pts with
multiple endocrine neoplasia INTERACTIONS
syndrome type 2 (MEN2). Unknown DRUG: Insulin, insulin secretagogues
if dulaglutide causes thyroid cell
tumors in humans. (e.g., glyBURIDE) may increase risk
Do not confuse dulaglutide with of hypoglycemia. HERBAL: None sig-
albiglutide or liraglutide. nificant. FOOD: None known. LAB VAL-
UES: Expected to decrease serum glucose,
uCLASSIFICATION Hgb A1c. May increase amylase, lipase.
PHARMACOTHERAPEUTIC: GLP-1
AVAILABILITY (Rx)
receptor agonist. CLINICAL: Antidia-
betic. Prefilled Injector Pen or Syringe: 0.75
mg/0.5 mL, 1.5 mg/0.5 mL.

USES ADMINISTRATION/HANDLING
Adjunct to diet and exercise to improve SQ
glycemic control in pts with type 2 dia- • Administer any time of day, without
betes mellitus. regard to food, on same day each
week. • May change administration day if
PRECAUTIONS last dose was given more than 3 days prior.
Contraindications: Hypersensitivity to If dose missed, administer within 3 days of
dulaglutide, other GLP-1 receptor ago- missed dose. If more than 3 days have
nists. Personal/family history of med- passed after missed dose, wait until next
ullary thyroid carcinoma or multiple regularly scheduled dose to administer.
endocrine neoplasia syndrome type Administration • Subcutaneously
2. Cautions: Pts with increased serum insert needle into abdomen, thigh,
calcitonin, thyroid nodules, hx pancre- or upper arm region and inject solu-
atitis, renal/hepatic impairment. Not tion. • Do not reuse needle. • Rotate
recommended in pts with severe GI injection sites each week.
disease, diabetic ketoacidosis, or type Storage • Refrigerate unused pens/
1 diabetes. syringes; do not freeze. • May store at
room temperature for up to 14
ACTION days. • Protect from light.
Activates GLP-1 receptors in pancreatic beta INDICATIONS/ROUTES/DOSAGE
cells. Therapeutic Effect: Augments glu-
cose-dependent insulin release, slows gas- Type 2 Diabetes Mellitus
tric emptying. Improves glycemic control. SQ: ADULTS/ELDERLY: Initially, 0.75 mg
once wkly. May increase to 1.5 mg once
PHARMACOKINETICS wkly if glycemic response inadequate.
Readily absorbed following SQ admin- Maximum: 1.5 mg wkly.
istration. Degraded into amino acids by Dose Modification
general protein catabolism. Peak plasma Concomitant use with insulin secre-
concentration: 24–72 hrs. Steady state tagogue (e.g., sulfonylurea) or insu-
reached in 2–4 wks. Elimination not lin: Consider reduced dose of insulin
specified. Half-life: 5 days.
underlined – top prescribed drug
DULoxetine 377
secretagogue or insulin based on glyce- actions, including diarrhea, gastropare-
mic goal. sis, vomiting. Screen for thyroid tumors
(dysphagia, dyspnea, persistent hoarse-
Dosage in Renal Impairment
ness, neck mass). If tumor suspected,
No dose adjustment. consider endocrinologist consultation.
Dosage in Hepatic Impairment Clinical significance of serum calcitonin D
Use caution. level or thyroid ultrasound with GLP-1–
associated thyroid tumors is debated/
SIDE EFFECTS unknown. Assess for hypoglycemia, hy-
Occasional (12%–6%): Nausea, diarrhea, perglycemia, hypersensitivity/allergic
vomiting, abdominal pain. Rare (4% or reaction. Screen for glucose-altering con-
less): Decreased appetite, dyspepsia, ditions: fever, stress, surgical procedures,
fatigue, asthenia. trauma. Obtain dietary consult for nutri-
tional education. Encourage PO intake.
ADVERSE EFFECTS/
TOXIC REACTIONS PATIENT/FAMILY TEACHING

May increase risk of acute renal failure or • Diabetes requires lifelong control.
worsening of chronic renal impairment Diet and exercise are principal parts of
(esp. with dehydration), severe gastropa- treatment; do not skip or delay meals.
resis, pancreatitis, thyroid C-cell tumors. Test blood sugar regularly. Monitor daily
May increase risk of hypoglycemia when calorie intake. • When taking addi-
used with other hypoglycemic agents or tional medications to lower blood sugar
insulin. Dyspnea, pruritus, rash may indi- or when glucose demands are altered
cate hypersensitivity reaction. May prolong (fever, infection, stress, trauma), have
PR interval by 2–3 msec or may rarely low blood sugar treatment available
cause first-degree AV block, tachycardia. (glucagon, oral dextrose). • Report
Immunogenicity (antidulaglutide anti- suspected pregnancy or plans for breast-
body formation) reported. Some pts with feeding. • Therapy may increase risk
antibody formation also tested positive for of thyroid cancer; report lumps or swell-
antibodies to GLP-1 and human albumin. ing of the neck; hoarseness, shortness of
breath, trouble swallowing. • Persis-
NURSING CONSIDERATIONS tent, severe abdominal pain that radiates
to the back (with or without vomiting)
BASELINE ASSESSMENT may indicate acute pancreati-
Obtain baseline fasting glucose level, Hgb tis. • Rash, itching, hives may indicate
A1c, BMP. Question history of medullary allergic reaction.
thyroid carcinoma, multiple endocrine
neoplasia syndrome type 2, pancreatitis,
renal impairment; first-degree AV block,
PR interval prolongation. Receive full med- DULoxetine
ication history and screen for use of other
hypoglycemic agents or insulin. Assess du-lox-e-teen
pt’s understanding of diabetes manage- (Cymbalta, Drizalma Sprinkle,
ment, routine home glucose monitoring, Duloxetine DR )
medication self-administration. Assess j BLACK BOX ALERT jIncreased
hydration status. risk of suicidal thinking and behav-
ior in children, adolescents, young
INTERVENTION/EVALUATION adults 18–24 yrs with major depres-
Monitor capillary blood glucose levels, sive disorder, other psychiatric
Hgb A1c; renal function test in pts with disorders.
renal impairment reporting severe GI re- Do not confuse DULoxetine
with FLUoxetine or PARoxetine.
Canadian trade name Non-Crushable Drug High Alert drug
378 DULoxetine
uCLASSIFICATION in liver. Excreted in urine (70%), feces
PHARMACOTHERAPEUTIC: Seroto- (20%). Half-life: 8–17 hrs.
nin norepinephrine reuptake inhibi-
LIFESPAN CONSIDERATIONS
tor (SNRI). CLINICAL: Antidepres-
sant. Pregnancy/Lactation: May produce
D neonatal adverse reactions (constant cry-
ing, feeding difficulty, hyperreflexia, irri-
USES tability). Unknown if distributed in breast
Treatment of major depression. Manage- milk. Breastfeeding not recommended.
ment of pain associated with diabetic Children: Safety and efficacy not estab-
neuropathy or chronic musculoskeletal lished. Elderly: Caution required when
pain. Treatment of generalized anxiety increasing dosage.
disorder. Treatment of fibromyalgia. OFF-
LABEL: Treatment of stress urinary incon-
INTERACTIONS
tinence in women. DRUG: Alcohol increases risk of hepatic
injury. CYP1A2 and CYP2D6 inhibi-
PRECAUTIONS tors (e.g., FLUoxetine, fluvoxaMINE,
Contraindications: Hypersensitivity PARoxetine) may increase plasma con-
to DULoxetine. Uncontrolled narrow- centration. MAOIs may cause serotonin
angle glaucoma. Use of MAOI intended syndrome (autonomic hyperactivity, coma,
to treat psychiatric disorder (concur- diaphoresis, excitement, hyperthermia,
rent or within 14 days of discontinuing rigidity). Aspirin, NSAIDs (e.g., ibu-
MAOI). Initiation of MAOI intended to profen, ketorolac, naproxen) may
treat psychiatric disorder within 5 days increase risk of bleeding. May increase
of discontinuing DULoxetine. Initiation of concentration, potential toxicity of tri-
DULoxetine in pt receiving linezolid or IV cyclic antidepressants. HERBAL: Glu-
methylene blue. Cautions: Renal impair- cosamine, herbs with anticoagulant/
ment, history of alcoholism, chronic antiplatelet properties (e.g., garlic,
hepatic disease, history of mania, pts with ginger, ginkgo biloba) may increase
suicidal ideation or behavior. Concurrent effect. FOOD: None known. LAB VAL-
use with inhibitors of CYP1A2 or thiorida- UES: May increase serum bilirubin, ALT,
zine, CNS depressants. Hypertension, con- AST, alkaline phosphatase.
trolled narrow-angle glaucoma, pts with
impaired GI motility. Concomitant use of AVAILABILITY (Rx)
NSAIDs (may increase risk of bleeding), Capsules (Delayed-Release, Enteric-
history of seizures. Use of medications Coated Pellets): 20 mg, 30 mg, 40 mg, 60
that lower seizure threshold; elderly; pts mg. (Drizalma Sprinkle): 20 mg, 30 mg, 40
at high risk for suicide. mg, 60 mg delayed-release capsules.
ACTION
ADMINISTRATION/HANDLING
Appears to inhibit serotonin and nor-
epinephrine reuptake at CNS neuronal b ALERT c Allow at least 14 days to
presynaptic membranes; is a less potent elapse between use of MAOIs and DULox-
inhibitor of DOPamine reuptake. Thera- etine.
peutic Effect: Produces antidepressant PO
effect. • Give without regard to food. Give with
PHARMACOKINETICS food, milk if GI distress occurs. • Do
Well absorbed from GI tract. Protein not break, crush, cut delayed-release
binding: greater than 90%. Metabolized capsules. • Contents of capsule may be

underlined – top prescribed drug


dupilumab 379
sprinkled on applesauce or mixed in ADVERSE EFFECTS/TOXIC
apple juice and swallowed (without REACTIONS
chewing) immediately. May slightly increase heart rate. Colitis,
dysphagia, gastritis, irritable bowel syn-
INDICATIONS/ROUTES/DOSAGE drome occur rarely.
D
Fibromyalgia
PO: ADULTS, ELDERLY: Initially, 30 mg/ NURSING CONSIDERATIONS
day for 1 wk. Increase to 60 mg/day. BASELINE ASSESSMENT
Assess appearance, behavior, speech pat-
Major Depressive Disorder
tern, level of interest, mood, sleep pat-
PO: ADULTS, ELDERLY: Initially, 40–60
tern, suicidal tendencies. Question pain
mg/day in 1 or 2 divided doses. For doses
level, intensity, location of pain.
greater than 60 mg/day, titrate in incre-
ments of 30 mg/day over 1 wk. Maxi- INTERVENTION/EVALUATION
mum: 120 mg/day. For pts on long-term therapy, serum chem-
istry profile to assess hepatic/renal function
Diabetic Neuropathy Pain
should be performed periodically. Super-
PO: ADULTS, ELDERLY: 60 mg once daily.
vise suicidal-risk pt closely during early
Maximum: 60 mg/day. Consider lower
therapy (as depression lessens, energy level
dose with renal impairment or if toler-
improves, increasing suicide potential).
ability is a concern.
Monitor B/P, mental status, anxiety, social
Generalized Anxiety Disorder functioning, serum glucose levels.
PO: ADULTS, ELDERLY: Initially, 30–60 PATIENT/FAMILY TEACHING
mg once daily. May increase up to 120
mg/day in 30-mg increments wkly. CHIL- • Therapeutic effect may be noted
DREN 7–17 YRS: Initially, 30 mg once
within 1–4 wks. • Do not abruptly dis-
daily. After 2 wks, may increase to 60 mg continue medication. • Avoid tasks that
once daily. May further increase in incre- require alertness, motor skills until re-
ments of 30 mg/day at wkly intervals. sponse to drug is established. • Inform
Maximum: 120 mg/day. physician of intention of pregnancy or if
pregnancy occurs. • Report anxiety,
Chronic Musculoskeletal Pain agitation, panic attacks, worsening of de-
PO: ADULTS, ELDERLY: 30 mg once daily pression. • Avoid heavy alcohol intake
for 1 wk, then increase to 60 mg once (associated with severe hepatic injury).
daily. Maximum: 60 mg/day.
Dosage in Renal/Hepatic Impairment
Renal: Not recommended with CrCl less
than 30 mL/min or ESRD. Hepatic: Not
dupilumab
recommended. doo-pil-ue-mab
(Dupixent)
SIDE EFFECTS
Do not confuse dupilumab with
Frequent (20%–11%): Nausea, dry mouth, belimumab, daclizumab, deno-
constipation, insomnia. Occasional (9%– sumab or durvalumab.
5%): Dizziness, fatigue, diarrhea, drowsi-
ness, anorexia, diaphoresis, vomiting. uCLASSIFICATION
Rare (4%–2%): Blurred vision, erectile PHARMACOTHERAPEUTIC: Interleu-
dysfunction, delayed or failed ejacula- kin-4 alpha antagonist. Monoclonal
tion, anorgasmia, anxiety, decreased antibody. CLINICAL: Anti-inflamma-
libido, hot flashes. tory.

Canadian trade name Non-Crushable Drug High Alert drug


380 dupilumab

USES INTERACTIONS
Treatment of moderate to severe atopic DRUG: May enhance the adverse/toxic
dermatitis in adults and pediatric pts 12 effects of live virus vaccines, beli-
yrs and older whose disease is not ade- mumab. HERBAL: None significant.
quately controlled with topical prescrip- FOOD: None known. LAB VALUES: May
D tion therapies or when those therapies are increase eosinophils.
not advisable. May be used with or with-
out corticosteroids. Add-on maintenance AVAILABILITY (Rx)
treatment of asthma in adults and pts 12 200 mg/1.14 mL,
Injection, Solution:
yrs and older with an eosinophilic pheno- 300 mg/2 mL in prefilled syringe.
type or corticosteroid-dependent asthma.
Add-on maintenance treatment in adults ADMINISTRATION/HANDLING
with inadequately controlled chronic rhi- SQ
nosinusitis with nasal polyposis. Preparation • Remove prefilled
syringe from refrigerator and allow to
PRECAUTIONS warm to room temperature (approx. 45
Contraindications: Hypersensitivity to mins) with needle cap intact. • Visually
dup­ilumab. Cautions: History of her- inspect for particulate matter or discolor-
pes simplex infection, parasitic (hel- ation. Solution should appear clear to
minth) infection. Safety and efficacy not slightly opalescent, colorless to pale yel-
established in the treatment of asthma. low in color. Do not use if solution is
Avoid use of live vaccines. cloudy, discolored, or if visible particles
are observed.
ACTION Administration • Insert needle sub-
Binds to the IL-4Ra subunit inhibiting cutaneously into upper arms, outer thigh,
interleukin-4 (IL-4) and interleukin-13 or abdomen, and inject solution. • Do
(IL-13), signaling cytokine-induced not inject into areas of active skin disease
responses, including release of pro- or injury such as sunburns, skin rashes,
inflammatory cytokines. Mechanism inflammation, skin infections, or active
of action in asthma not established. psoriasis. • Rotate injection sites.
Therapeutic Effect: Reduces skin Storage • Refrigerate in original
inflammation. carton until time of use. • May be
stored at room temperature for up to
PHARMACOKINETICS 14 days. • Protect from light. • Do
Widely distributed. Degraded into small not freeze or expose to external heat
peptides and amino acids via catabolic sources. • Do not shake.
pathway. Peak plasma concentration:
7 days. Steady state reached by wk 16. INDICATIONS/ROUTES/DOSAGE
Excretion/clearance: time to nonde- Atopic Dermatitis
tectable concentration: 10 wks. Half- SQ: ADULTS, ELDERLY: Initially, 600 mg
life: Not specified. (two 300-mg injections at different sites),
then 300 mg every other week. If a dose
LIFESPAN CONSIDERATIONS is missed, administer within 7 days of
Pregnancy/Lactation: Unknown if missed dose, then resume normal sched-
distributed in breast milk. However, ule. If missed dose is not within 7 days,
human immunoglobulin G (IgG) is pres- wait until next scheduled dose. CHILDREN
ent in breast milk and is known to cross 12 YRS AND OLDER, ADOLESCENTS 17 YRS
the placenta. Children: Safety and effi- OR YOUNGER, WEIGHING 60 KG OR MORE:
cacy not established. Elderly: No age- Initially, 600 mg once (administered as
related precautions noted. two 300-mg injections), followed by a
maintenance dose of 300 mg q2wks.
underlined – top prescribed drug
dupilumab 381
WEIGHING LESS THAN 60 KG: Initially, 400 NURSING CONSIDERATIONS
mg once (administered as two 200-mg
injections), followed by a maintenance BASELINE ASSESSMENT
dose of 200 mg q2wks. Question history of herpes zoster infec-
Asthma (Moderate to Severe) tion, parasitic infection, hypersensitiv-
ity reaction. Question recent adminis- D
SQ: ADULTS, ELDERLY, CHILDREN 12 YRS
AND OLDER: Initially, 400 mg (give as two tration of live virus vaccine. Pts with
200-mg injections) or 600 mg (give as preexisting helminth (parasite) infec-
two 300-mg injections). Maintenance: tion should be treated prior to first
200 mg (following initial 400-mg dose) dose. Inhaled or systemic corticoste-
or 300 mg (following initial 600-mg roids should not be suddenly discon-
dose) every other wk. tinued upon initiation. Conduct derma-
tologic exam; record characteristics of
Asthma (Steroid-Dependent or with psoriatic lesions. Consider administra-
Atopic Dermatitis) tion of age-appropriate immunizations
SQ: ADULTS, ELDERLY, CHILDREN 12 YRS (if applicable) before initiation. Assess
AND OLDER: Initially, 600 mg, then 300 pt’s willingness to self-inject medica-
mg every other wk. tion.
Rhinosinusitis (Chronic) with Nasal INTERVENTION/EVALUATION
Polyposis Interrupt or discontinue treatment if
SQ: ADULTS, ELDERLY: 300 mg every other hypersensitivity reaction, opportunistic
wk. infection (esp. parasite infection, herpes
Dosage in Renal/Hepatic Impairment zoster infection), worsening of asthma-
No dose adjustment (not studied). related symptoms (esp. in pts tapering
off corticosteroids) occurs. Concomitant
SIDE EFFECTS use of topical calcineurin inhibitors is
Occasional (10%): Injection site reac- allowed, but only for areas that remain
tions, eye inflammation/irritation. Rare problematic (face, neck, genitals, skin
(1%): Eye pruritus, dry eye. folds). Assess for improvement of skin
lesions.
ADVERSE EFFECTS/
TOXIC REACTIONS PATIENT/FAMILY TEACHING
Hypersensitivity reactions including • A health care provider will show you
serum sickness (arthralgia, itch- how to properly prepare and inject your
ing, glomerulonephritis, hypotension, medication. You must demonstrate cor-
lymphadenopathy, malaise, proteinuria, rect preparation and injection tech-
pyrexia, rash, shock, splenomegaly), niques before using medication at
urticaria reported in less than 1% of home. • Inject medication into your
pts, which correlated with high antibody outer thigh or abdomen; caregivers may
titers. Blepharitis, conjunctivitis (aller- also inject medication in the outer
gic, bacterial, giant papillary, viral), arm. • Immediately report allergic re-
keratitis (ulcerative, allergic, atopic actions such as difficulty breathing,
keratoconjunctivitis), herpes simplex itching, hives, rash, swelling of the face
infection (genital, otitis externa, herpes or tongue. • Report infections of any
virus infection) may occur. Unknown if kind. • Do not stop corticosteroid
treatment will influence the immunologic therapy unless directed by pre-
response to helminth (parasite) infec- scriber. • Do not receive live vac-
tion. Immunogenicity (auto-dupilumab cines. • Do not interrupt or stop
antibodies) reported in 7% of pts. asthma medications or treatments.

Canadian trade name Non-Crushable Drug High Alert drug


382 durvalumab
activation allowing T-cells to kill tumor
durvalumab cells. Restores antitumor T-cell function.
Therapeutic Effect: Inhibits tumor cell
dur-val-ue-mab growth and metastasis.
(Imfinzi)
D Do not confuse durvalumab PHARMACOKINETICS
with daclizumab, dupilumab, or Widely distributed. Metabolism not
nivolumab. specified. Steady state reached in 16 wks.
Excretion not specified. Half-life: 17
uCLASSIFICATION
days.
PHARMACOTHERAPEUTIC: Anti-
programmed death ligand-1 (PD-L1). LIFESPAN CONSIDERATIONS
Monoclonal antibody. CLINICAL: Pregnancy/Lactation: Avoid preg-
Antineoplastic. nancy; may cause fetal harm. Females
of reproductive potential should use
effective contraception during treatment
USES
and for at least 3 mos after discontinu-
Treatment of pts with locally advanced or ation. Unknown if distributed in breast
metastatic urothelial carcinoma who have milk; however, human immunoglobulin
disease progression during or following G (IgG) is present in breast milk and is
platinum-containing chemotherapy or known to cross the placenta. Breastfeed-
have disease progression within 12 mos ing not recommended during treatment
of neoadjuvant or adjuvant treatment and for at least 3 mos after discon-
with platinum-containing chemotherapy. tinuation. Children: Safety and efficacy
Treatment of unresectable stage III non– not established. Elderly: May have
small-cell lung cancer (NSCLC) that has increased risk of toxic reactions; use
not progressed following concurrent caution.
platinum-based chemotherapy and radia-
tion therapy. INTERACTIONS
DRUG: May enhance adverse effects/
PRECAUTIONS
toxicity of belimumab. HERBAL: None
Contraindications: Hypersensitivity to significant. FOOD: None known. LAB
durvalumab. Cautions: Active infection, VALUES: May increase serum albumin,
conditions predisposing to infection alkaline phosphatase, ALT, AST, bilirubin,
(e.g., diabetes, immunocompromised calcium, creatinine, glucose, magne-
pts, renal failure, open wounds); corti- sium. May decrease serum sodium; Hgb,
costeroid intolerance, baseline hema- Hct, lymphocytes, neutrophils, RBCs. May
tologic cytopenias, elderly pts, hepatic increase or decrease serum potassium.
impairment, interstitial lung disease,
renal insufficiency; history of autoim- AVAILABILITY (Rx)
mune disorders (Crohn’s disease, 120 mg/2.4 mL (50 mg/mL),
Injection:
demyelinating polyneuropathy, Guillain- 500 mg/10 mL (50 mg/mL).
Barré syndrome, Hashimoto’s thyroid-
itis, hyperthyroidism, myasthenia gravis, ADMINISTRATION/HANDLING
rheumatoid arthritis, Type I diabetes, IV
vasculitis); diabetes, pancreatitis.
Preparation • Visually inspect vial for
ACTION particulate matter or discoloration. Solu-
Blocks programmed cell death ligand tion should appear clear to opalescent,
1 (PD-L1) binding to PD-1 and CD80 colorless to slightly yellow in color. • Do
(B7.1). PD-L1 blockade increases T-cell not use if solution is cloudy, discolored,

underlined – top prescribed drug


durvalumab 383
or if visible particles are observed. • Do Colitis (GI Toxicity)
not shake. • Withdraw proper volume Grade 2 diarrhea or colitis: Withhold
from vial and dilute in 0.9% NaCl or D5W dose. Start predniSONE 1–2 mg/kg/day
to a final concentration of 1–15 mg/ (or equivalent) followed by taper. Grade
mL. • Gently invert to mix; do not 3 or 4 diarrhea or colitis: Permanently
shake. • Diluted solution should appear discontinue. Start predniSONE 1–2 mg/ D
clear, colorless, and free of particles. kg/day (or equivalent), followed by taper.
Rate of administration • Infuse over
Dermatitis
60 mins via dedicated IV line using a
Grade 2 rash or dermatitis (for greater
sterile, low protein-binding 0.2- or
than 1 wk); Grade 3 rash or dermati-
0.22-micron in-line filter.
tis: Withhold dose. Consider starting pred-
Storage • Refrigerate unused vials in
original carton. • Protect from light. niSONE 1–2 mg/kg/day (or equivalent),
May refrigerate diluted solution for no followed by taper. Grade 4 rash or der-
matitis: Permanently discontinue. Con-
more than 24 hrs or store at room tem-
perature for no more than 4 hrs. If sider starting predniSONE 1–2 mg/kg/day
refrigerated, allow diluted solution to (or equivalent), followed by taper.
warm to room temperature before Endocrinopathies
use. • Do not freeze or shake. Grade 2–4 adrenal insufficiency
(hypophysitis, hypopituitarism): With-
IV INCOMPATIBILITIES hold dose until clinically stable. Start pred-
Do not infuse with other medications. niSONE 1–2 mg/kg/day (or equivalent),
followed by taper. Consider hormone
INDICATIONS/ROUTES/DOSAGE replacement therapy as clinically indicated.
Urothelial Carcinoma Grade 2–4 hyperthyroidism: Withhold
IV: ADULTS, ELDERLY: 10 mg/kg q2wks. dose until clinically stable and manage symp-
Continue until disease progression or toms. Grade 2–4 hypothyroidism: Con-
unacceptable toxicity. sider hormone replacement therapy. Grade
2–4 type 1 diabetes: Withhold dose until
NSCLC clinically stable. Start insulin therapy as
IV: ADULTS, ELDERLY: 10 mg/kg q2wks. clinically indicated.
Continue until disease progression or
unacceptable toxicity or maximum of 12 Hepatitis (Hepatotoxicity During
mos. Treatment)
Grade 2 hepatitis (serum ALT or
Dose Modification AST greater than 3 and up to 5
Note: Withhold and/or discontinue dur- times upper limit of normal [ULN] or
valumab to manage adverse reactions. serum bilirubin greater than 1.5 and
Based on severity of adverse reactions, up to 3 times ULN); Grade 3 hepati-
withhold durvalumab and administer tis (serum ALT or AST less than or
systemic corticosteroids. Initiate corti- equal to 8 times ULN or serum bili-
costeroid taper when adverse reactions rubin less than or equal to 5 times
improve to below Grade 1, and continue ULN): Withhold dose. Start predniSONE
taper over at least 1 mo. If treatment is not 1–2 mg/kg/day (or equivalent), followed
permanently discontinued due to adverse by taper. Grade 3 hepatitis (serum
reactions, resume therapy when adverse ALT or AST greater than 8 times
reactions return to Grade 1 or lower and ULN or serum bilirubin greater than
the corticosteroid dose has been reduced 5 times ULN; transaminase eleva-
to less than 10 mg predniSONE (or tion (concurrent serum ALT or AST
equivalent) per day. No dose reductions greater than 3 times ULN and serum
of durvalumab are recommended. bilirubin greater than 2 times ULN)

Canadian trade name Non-Crushable Drug High Alert drug


384 durvalumab
with no known cause: Permanently pain, myalgia, constipation, decreased
discontinue. Start predniSONE 1–2 mg/ appetite. Occasional (16%–11%): Nau-
kg/day (or equivalent), followed by taper. sea, peripheral edema, scrotal edema,
lymphedema, abdominal/flank pain,
Infection diarrhea, pyrexia, dyspnea, cough, der-
D Grade 3 or 4 infection: Withhold dose matitis, dermatitis acneiform, dermatitis
and manage symptoms. Start anti-infectives psoriasiform, psoriasis, maculopapular
for suspected or confirmed infections. rash, pustular rash, eczema, erythema,
Infusion-Related Reactions erythema multiforme, erythematous rash,
Grade 1 or 2 infusion reactions: Inter- acne, lichen planus.
rupt or decrease rate of infusion. Consider ADVERSE EFFECTS/TOXIC
premedication for subsequent infusions. REACTIONS
Grade 3 or 4 infusion reactions: Per-
manently discontinue. Anemia, neutropenia, lymphopenia are
expected responses to therapy. May
Nephritis (Renal Toxicity During cause severe, sometimes fatal immune-
Treatment) mediated reactions such as adrenal
Grade 2 nephritis (serum creatinine insufficiency (1% of pts), colitis (2% of
greater than 1.5 and up to 3 times pts), hepatitis (1% of pts), hypothyroid-
ULN): Withhold dose. Start predniSONE ism (9% of pts), hyperthyroidism (6% of
1–2 mg/kg/day (or equivalent), followed pts), hypophysitis, nephritis (less than 1%
by taper. Grade 3 nephritis (serum of pts), pneumonitis (2% of pts), type 1
creatinine greater than 3 and up diabetes (less than 1% of pts), rash (15%
to 6 times ULN); Grade 4 nephritis of pts); aseptic meningitis, hemolytic
(serum creatinine greater than 6 anemia, keratitis, myocarditis, myositis,
times ULN): Permanently discontinue. thrombocytopenic purpura, uveitis. Uri-
Start predniSONE 1–2 mg/kg/day (or nary tract infections including candiduria,
equivalent), followed by taper. cystitis, urosepsis occurred in 15% of pts.
Immunogenicity (auto-durvalumab anti-
Other Toxic Reactions bodies) reported in 3% of pts.
Any other Grade 3 reactions: With-
hold dose and manage symptoms. Any NURSING CONSIDERATIONS
other Grade 4 reactions: Permanently
discontinue. Start predniSONE 1–4 mg/ BASELINE ASSESSMENT
kg/day (or equivalent), followed by taper. Obtain CBC, BMP, LFT, serum ionized
calcium, magnesium; thyroid func-
Pneumonitis
tion test; urine pregnancy; vital signs.
Grade 2 pneumonitis: Withhold dose. Question medical history as listed in
Start predniSONE 1–2 mg/kg/day (or Precautions; prior infusion reactions.
equivalent), followed by taper. Grade Question intolerance to corticoste-
3 or Grade 4 pneumonitis: Perma-
roids. Verify use of effective contracep-
nently discontinue. Start predniSONE tion in females of reproductive poten-
1–4 mg/kg/day (or equivalent) followed tial. Screen for active infection. Assess
by taper. nutritional/hydration status. Conduct
Dosage in Renal/Hepatic Impairment neurologic/dermatologic exam. Offer
(Prior to Treatment Initiation) emotional support.
Not specified; use caution.
INTERVENTION/EVALUATION
SIDE EFFECTS Monitor CBC, BMP, LFT, serum ionized
Frequent (39%–19%): Fatigue, asthenia, calcium, magnesium; thyroid function
malaise, back/musculoskeletal/neck test periodically. Monitor for infusion

underlined – top prescribed drug


duvelisib 385
reactions including angioedema, back colored/tarry stools, yellowing of skin or
or neck pain, dyspnea, flushing, pru- eyes), nerves (severe nerve pain or loss
ritus, pyrexia, rash, syncope. Consider of motor function), pituitary (persistent
increasing corticosteroid dose if toxic or unusual headache, dizziness, extreme
effects worsen or do not improve. Assess weakness, fainting, vision changes), thy-
skin for rash, lesions. Diligently moni- roid (trouble sleeping, high blood pres- D
tor for immune-mediated adverse effects sure, fast heart rate [overactive thyroid]
as listed in Adverse Effects/Toxic Reac- or fatigue, goiter, weight gain [underac-
tions. Notify physician if any CTCAE tox- tive thyroid]). Immediately report infu-
icities occur and initiate proper treat- sion reactions such as neck or back pain,
ment. If immune-mediated reactions dizziness, fever, flushing, itching, short-
occur, consider referral to specialist. ness of breath, swelling of the
Obtain CXR if interstitial lung disease, face. • Treatment may cause severe di-
pneumonitis suspected. Interrupt or dis- arrhea. Drink plenty of fluids.
continue treatment if serious ­infection,
­opportunistic infection, sepsis occurs,
and initiate appropriate antimicrobial
therapy. If corticosteroid therapy is duvelisib
started, monitor capillary blood glucose
and screen for corticosteroid side ef- doo-ve-lis-ib
fects or intolerance. Report neurologic (Copiktra)
changes including nuchal rigidity with j BLACK BOX ALERT j Fatal
fever, positive Kernig’s sign, positive and/or serious infections reported
Brudzinski’s sign, altered mental status, in 31% of pts. Monitor for symptoms
seizures (related to aseptic meningitis). of infection. Fatal and/or serious
diarrhea or colitis reported in 18%
Strictly monitor I&O. Encourage fluid of pts. Monitor for GI symptoms.
intake. Fatal and/or serious pneumonitis
reported 5% of pts. Monitor for
PATIENT/FAMILY TEACHING pulmonary symptoms and intersti-
• Treatment may depress your immune tial infiltrates. Fatal and/or serious
cutaneous reported occurred in
system and reduce your ability to fight 5% of pts.
infection. Report symptoms of infection Do not confuse Copiktra with
such as body aches, chills, cough, fa- Cometriq; duvelisib with co-
tigue, fever. Avoid those with active infec- panlisib, dabrafenib, dasatinib,
tion. • Avoid pregnancy; treatment may durvalumab, or idelalisib.
cause birth defects. Do not breastfeed.
Females of childbearing potential should uCLASSIFICATION
use effective contraception during treat- PHARMACOTHERAPEUTIC: Phos-
ment and for at least 3 mos after final phatidylinositol-3-kinase inhibitor.
dose. • Treatment may cause serious CLINICAL: Antineoplastic.
or life-threatening inflammatory reac-
tions. Report signs and symptoms of
treatment-related inflammatory events in
the following body systems: brain (confu- USES
sion, headache, fever, rigid neck, sei- Treatment of relapsed or refractory
zures), colon (severe abdominal pain or chronic lymphocytic leukemia (CLL) or
diarrhea), eye (blurry vision, double vi- small lymphocytic lymphoma (SLL) after
sion, unequal pupil size, sensitivity to at least two prior therapies. Treatment of
light, drooping eyelid), lung (chest pain, relapsed or refractory follicular lym-
cough, shortness of breath), liver (bruis- phoma after at least two prior systemic
ing easily, amber-colored urine, clay- therapies.

Canadian trade name Non-Crushable Drug High Alert drug


386 duvelisib

PRECAUTIONS decrease concentration/effect. May decrease


Contraindications: Hypersensitivity to efficacy of BCG (intravesical), vaccines
duvelisib. Cautions: Baseline anemia, (live). May increase adverse effects of vac-
leukopenia, lymphopenia, neutropenia, cines (live). HERBAL: St. John’s wort
thrombocytopenia; active infection, con- may decrease concentration/effect. Echina-
D ditions predisposing to infection (e.g., cea may decrease therapeutic effect. FOOD:
diabetes, renal failure, immunocompro- Grapefruit products may increase con-
mised pts, open wounds), dehydration, centration/effect. LAB VALUES: May increase
hepatic impairment, history of pulmo- serum alkaline phosphatase, amylase, ALT,
nary disease. Concomitant use of strong AST, creatinine, lipase, potassium. May
CYP3A inducers or CYP3A inhibitors. decrease serum albumin, calcium, sodium,
phosphate; absolute neutrophil count
ACTION (ANC), Hct, Hgb, leukocytes, lymphocytes,
Inhibits phosphatidylinositol-3-kinase neutrophils, platelets, RBC count.
(PI3K) expressed on malignant B-cells.
AVAILABILITY (Rx)
Inhibits signaling pathway of B-cell
receptors, lymphoma cells lines, and Capsules: 15 mg, 25 mg.
CXCR12-mediated chemotaxis of malig-
ADMINISTRATION/HANDLING
nant B-cells. Therapeutic Effect: Inhib-
its tumor cell growth and metastasis. PO
• Give without regard to food. • Admin-
PHARMACOKINETICS ister whole; do not break, cut, or open
Widely distributed. Metabolized in liver. capsule. Capsule cannot be chewed. • If
Protein binding: 98%. Peak plasma con- a dose is missed by no more than 6 hrs,
centration: 1–2 hrs. Excreted in feces administer as soon as possible. If a dose
(79%), urine (14%). Half-life: 4.7 hrs. is missed by more than 6 hrs, skip dose
and administer at next regularly sched-
LIFESPAN CONSIDERATIONS uled time.
Pregnancy/Lactation: Avoid pregnancy;
INDICATIONS/ROUTES/DOSAGE
may cause fetal harm. Female pts of repro-
ductive potential must use effective contra- NOTE: Recommend prophylactic ther-
ception during treatment and for at least 1 apy for Pneumocystis jirovecii pneumo-
mo after discontinuation. Unknown if dis- nia (PJP) during treatment and until ab-
tributed in breast milk. Breastfeeding not solute CD4+ T-cell count is greater than
recommended during treatment and for 200 cells/mm3. To prevent cytomegalovi-
at least 1 mo after discontinuation. Men: rus (CMV) infection, recommend pro-
Male pts with female partners of reproduc- phylactic antiviral therapy during treat-
tive potential must use effective contracep- ment.
tion (e.g., condoms) during treatment and
CLL, SLL, Follicular Lymphoma
for at least 1 mo after discontinuation.
PO: ADULTS, ELDERLY: 25 mg twice daily
May impair fertility. Children: Safety and
of 28-day cycle.
efficacy not established. Elderly: No age-
related precautions noted. Reduction Schedule for Adverse Effects
First dose reduction: 15 mg. Un-
INTERACTIONS able to tolerate 15 mg dose: Permanently
DRUG: Strong CYP3A4 inhibitors (e.g., discontinue.
clarithromycin, ketoconazole) may
increase concentration/effect. Strong Dose Modification
CYP3A4 inducers (e.g., carbam- Based on Common Terminology Criteria
azepine, phenytoin, rifAMPin) may for Adverse Events (CTCAE).

underlined – top prescribed drug


duvelisib 387
Cutaneous Reactions (confirmed with positive PCR test or
Grade 1 or 2 cutaneous reac- antigen test): Withhold treatment until
tions: Maintain dose and treat with sup- resolved, then resume at same or reduced
portive therapy. Grade 3 cutaneous dose.
reactions: Withhold treatment until
resolved with supportive therapy, then Neutropenia D
resume at reduced dose. Life-threaten- ANC 500–1000 cells/mm3: Maintain
ing or recurrent cutaneous reactions, dose. ANC less than 500 cells/mm3:
Stevens-Johnson syndrome, toxic Withhold treatment until ANC is greater
epidermal necrolysis, drug reaction than 500 cells/mm3, then resume at same
with eosinophilia and systemic reac- dose for first occurrence or at reduced
tion: Permanently discontinue. dose for subsequent occurrence.

Diarrhea or Colitis (noninfectious) Thrombocytopenia


Grade 1 or 2 diarrhea that is respon- Platelet count 25,000 to less than
sive to antidiarrheal medication; 50,000 cells/mm3 with Grade 1
asymptomatic Grade 1 colitis: Maintain bleeding: Maintain dose. Platelet count
dose and treat with antidiarrheal medica- 25,000 to less than 50,000 cells/mm3
tion. Grade 1 or 2 diarrhea that is not with Grade 2 bleeding; platelet count
responsive to antidiarrheal medica- less than 25,000 cells/mm3: Withhold
tion: Withhold treatment until resolved treatment until platelet count is greater
with supportive therapy. Once resolved, than or equal to 25,000 cells/mm3 and
resume at reduced dose. Grade 3 diar- bleeding has resolved (if applicable).
rhea, abdominal pain, hematochezia, Resume at same dose for first occur-
stool with mucous, change in bowel rence or at reduced dose for subsequent
habits, peritoneal signs: Withhold treat- occurrence.
ment until resolved with supportive therapy,
then resume at reduced dose. Recurrent Pneumonitis (noninfectious)
Grade 3 diarrhea; recurrent colitis Grade 2 symptomatic pneumonitis:
(any grade): Permanently discontinue. Withhold treatment and treat pneumo-
nitis as appropriate. Once improved to
Hepatotoxicity Grade 1 or 0, resume at reduced dose.
Serum ALT/AST elevation 3–5 times Grade 3 pneumonitis; life-threat-
upper limit of normal (ULN): Main- ening or recurrent pneumonitis
tain dose. Serum ALT/AST elevation despite steroid therapy: Permanently
greater than 5–20 times ULN: With- discontinue.
hold treatment until serum ALT/AST less
than 3 times ULN, then resume at same Concomitant Use with Strong CYP3A
dose for first occurrence or at reduced Inhibitors
dose for subsequent occurrence. Serum If CYP3A inhibitor cannot be discontin-
ALT/AST elevation greater than 20 ued, reduce dose to 15 mg twice daily.
times ULN: Permanently discontinue.
Dosage in Renal/Hepatic Impairment
Infection Mild to severe impairment: Not speci-
Grade 3 or higher infection: Withhold fied; use caution.
treatment until resolved, then resume at
same or reduced dose. PJP infection SIDE EFFECTS
of any grade: Withhold treatment and Frequent (50%–13%): Diarrhea, rash,
evaluate for confirmation. If PJP infection fatigue, pyrexia, cough, nausea, musculo-
is confirmed, permanently discontinue. skeletal pain, abdominal pain, vomiting,
Clinical CMV infection or viremia mucositis, edema, decreased appetite,

Canadian trade name Non-Crushable Drug High Alert drug


388 duvelisib
constipation. Occasional (12%–10%): INTERVENTION/EVALUATION
Headache, dyspnea, arthralgia. Monitor ANC, CBC, LFT periodically. If
blood dyscrasias occurs, monitor ANC,
ADVERSE EFFECTS/TOXIC CBC wkly until improved. If hepatotoxic-
REACTIONS ity occurs, monitor LFTs wkly until im-
D Anemia, leukopenia, lymphopenia, lym- proved. Be alert for infections, esp. re-
phocytosis, neutropenia, thrombocyto- spiratory tract infection such as
penia is an expected response to ther- Pneumocystis jirovecii pneumonia,
apy. Serious infections including bacterial/fungal/pneumococcal/viral
pneumonia, bronchopulmonary asper- pneumonia (cough, dyspnea, hypoxia,
gillosis, sepsis, lung infection reported pleuritic chest pain). If infection occurs,
in 31% of pts. Pneumocystis jirovecii provide anti-infective therapy as appro-
pneumonia reported in less than 1% of priate. Consider ABG, radiologic test if
pts. CMV infection/reactivation or vire- ILD/pneumonitis (excessive cough, dys-
mia reported in 1% of pts. Fatal and/or pnea, hypoxia) is suspected. If treatment-
severe diarrhea or colitis reported in related toxicities occur, consider referral
18% of pts. Serious cutaneous reactions to specialist. Assess skin for cutaneous
including erythema, pruritus, rash, reactions, skin toxicities. Monitor for
toxic skin eruption, skin peeling, exfo- CMV reactivation (by PCR test or antigen
liation, keratinocyte necrosis occurred test) at least monthly in pts who test
in 5% of pts. Fatal cases of toxic epider- positive for CMV. In pts who develop diar-
mal necrolysis, drug reaction with eo- rhea, colitis, abdominal pain, or change
sinophilia and systemic reaction have in bowel habits, monitor daily pattern of
occurred. Noninfectious pneumonitis bowel activity and stool consistency at
occurred in 5% of pts. Grade 3 or 4 least wkly until resolved with supportive
hepatotoxicity reported in 2%–8% of therapies. In pts who develop cutaneous
pts. Grade 3 or 4 neutropenia reported reactions, monitor at least wkly until re-
in 42% of pts, which may greatly in- solved with supportive therapies. Moni-
crease risk of infection. tor I&Os, hydration status.
NURSING CONSIDERATIONS PATIENT/FAMILY TEACHING

BASELINE ASSESSMENT
• Treatment may depress your immune
system and reduce your ability to fight
Obtain ANC, CBC, LFTs; pregnancy test in infection. Report symptoms of infection
female pts of reproductive potential. such as body aches, chills, cough, fa-
Question current breastfeeding status. tigue, fever. Avoid those with active infec-
Confirm compliance of effective contra- tion. • Report symptoms of bone mar-
ception. Screen for active infection. Rec- row depression such as bruising, fatigue,
ommend prophylaxis therapy for Pneu- fever, shortness of breath, weight loss;
mocystis jirovecii pneumonia during bleeding easily, bloody urine or
treatment and until absolute CD4+ T cell stool. • Report symptoms of liver prob-
count is greater than 200 cells/mm3. To lems (abdominal pain, bruising, clay-
prevent CMV infection, recommend pro- colored stool, amber- or dark-colored
phylactic antiviral therapy during treat- urine, yellowing of the skin or eyes); in-
ment. Assess skin for open wounds, le- flammation of the lung (excessive cough,
sions. Assess hydration status. Question difficulty breathing, chest pain); toxic
history of hepatic impairment, pulmo- skin reactions (itching, peeling, rash,
nary disease. redness, swelling). • Female and male
Receive full medication history and pts of childbearing potential must use
screen for interactions. Offer emotional reliable contraception during treatment
support. and for at least 1 mo after last dose. Do

underlined – top prescribed drug


duvelisib 389
not breastfeed during treatment and for dration. • Drink plenty of fluids. • Do
at least 1 mo after last dose. • Treat- not take newly prescribed medications
ment may cause severe diarrhea, which unless approved by the prescriber who
may require antidiarrheal medication. originally started treatment. • Do not
Report worsening of diarrhea or dehy- ingest grapefruit products.
D

Canadian trade name Non-Crushable Drug High Alert drug


390 edoxaban
stroke); mechanical heart valves; moder-
edoxaban ate to severe mitral stenosis.

e-dox-a-ban ACTION
(Savaysa, Lixiana ) Selectively blocks active site of factor Xa,
j BLACK BOX ALERT j Avoid a key factor in the intrinsic and extrinsic
use in nonvalvular atrial fibrillation pathway of blood coagulation cascade.
E pts with creatinine clearance (CrCl) Inhibits platelet activation and fibrin clot
greater than 95 mL/min (increased formation. Therapeutic Effect: Inhib-
risk of ischemic stroke). Premature
discontinuation of oral anticoagu- its blood coagulation.
lant in the absence of alternative PHARMACOKINETICS
anticoagulation may increase risk of
ischemic events. If treatment is dis- Readily absorbed after PO administra-
continued for any reason other than tion. Peak plasma concentration: 1–2
pathologic bleeding or completion hrs. Steady state reached within 3 days.
of course of therapy, consider cov-
erage with another anticoagulant Protein binding: 55%. Primarily excreted
as described in transition guideline. in urine (50%), biliary/intestinal excre-
Epidural or spinal hematomas may tion (remaining %). Not removed by
occur in pts who are receiving hemodialysis. Half-life: 10–14 hrs.
neuraxial anesthesia or undergoing
spinal puncture, which may result in LIFESPAN CONSIDERATIONS
long-term or permanent paralysis.
Pregnancy/Lactation: Unknown if
Do not confuse edoxaban with
excreted in breast milk. Children: Safety
apixaban or rivaroxaban.
and efficacy not established. Elderly: May
uCLASSIFICATION have increased risk of bleeding due to age-
related renal impairment.
PHARMACOTHERAPEUTIC: Factor Xa
inhibitor. CLINICAL: Anticoagulant. INTERACTIONS
DRUG: NSAIDs (e.g., ibuprofen, ketor-
olac, naproxen), fibrinolytic therapy
USES (e.g., alteplase), aspirin may increase
To reduce risk of stroke and systemic concentration/effect; may increase risk
embolism (SE) in pts with nonvalvular atrial of bleeding. Strong CYP3A4 inducers
fibrillation (NVAF). Treatment of deep vein (e.g., carBAMazepine, phenytoin,
thrombosis (DVT) and pulmonary embo- rifAMPin) may decrease concentration/
lism (PE) following 5–10 days of initial effect. Apixaban, dabigatran, rivar-
therapy with a parenteral anticoagulant. oxaban may increase anticoagulant effect.
HERBAL: Herbals with anticoagulant/
PRECAUTIONS antiplatelet properties (e.g., garlic,
Contraindications: Hypersensitivity to ginger, ginkgo biloba) may increase
edoxaban. Major active bleeding. Cau- risk of bleeding. FOOD: None known. LAB
tions: Elderly, pts at increased risk of VALUES: May increase serum AST, ALT.
bleeding (e.g., prior CVA, thrombocy- May prolong aPTT, PT/INR.
topenia, severe uncontrolled hyperten-
sion; history of bleeding ulcers, upper or AVAILABILITY (Rx)
lower GI bleeding), recent surgery, renal/ Tablets: 15 mg, 30 mg, 60 mg.
hepatic impairment. Avoid concomitant
use with aspirin, heparin, low molecular ADMINISTRATION/HANDLING
weight heparin (LMWH), NSAIDs, P-gp PO
inducers (e.g., rifAMPin). Not recom- • Give without regard to food. • Do
mended in pts with CrCl greater than not administer within 2 hrs of removal of
95 mL/min (increased risk of ischemic epidural or intrathecal catheters.
underlined – top prescribed drug
edoxaban 391

INDICATIONS/ROUTES/DOSAGE start edoxaban at the time of the next


Nonvalvular Atrial Fibrillation scheduled dose of LMWH. From low
PO: ADULTS, ELDERLY: 60 mg once daily. unfractionated heparin: Discontinue
infusion and start edoxaban 4 hrs later.
DVT/PE
PO: ADULTS, ELDERLY WEIGHING MORE Transition Guideline from Edoxaban to
THAN 60 KG: 60 mg once daily following Other Anticoagulant
5–10 days of initial therapy with a par- To Warfarin: Oral option: For pts E
enteral anticoagulant. 60 KG OR LESS: 30 taking edoxaban 60 mg, reduce to 30 mg
mg once daily. and begin warfarin concomitantly. For pts
taking edoxaban 30 mg, reduce dose to
Dose Modification 15 mg and begin warfarin concomitantly.
Body weight less than or equal to Once stable INR greater than or equal to
60 kg or concomitant use of certain 2, discontinue edoxaban and continue
P-gp inhibitors: 30 mg once daily. warfarin. Parenteral option: Discon-
tinue edoxaban and administer paren-
Dosage in Renal Impairment teral anticoagulant and warfarin at the
DVT/PE time of next scheduled edoxaban dose.
CrCl 15–50 mL/min: 30 mg once daily. Once stable INR greater than or equal to
CrCl less than 15 mL/min: Not rec- 2, discontinue parenteral anticoagulant
ommended. and continue warfarin. To nonvitamin
K-­
dependent oral anticoagulant or
NVAF
parenteral anticoagulant: Discontinue
CrCl greater than 95 mL/min: Not
edoxaban and start other oral anticoagulant
recommended. CrCl 51–95 mL/min:
at the time of the next scheduled dose.
No dose adjustment. CrCl 15–50 mL/
min: 30 mg once daily. CrCl less than SIDE EFFECTS
15 mL/min: Not recommended. Rare (4%): Rash.
Dosage in Hepatic Impairment
ADVERSE EFFECTS/TOXIC
Mild impairment: No dose adjustment.
REACTIONS
Moderate to severe impairment: Not
recommended. Hemorrhagic events including intracranial
hemorrhage, hemorrhagic stroke, cuta-
Discontinuation for Surgery or Other neous/GI/GU/oral/pharyngeal/urethral/
Interventions vaginal bleeding, epistaxis, epidural/spinal
Discontinue at least 24 hrs before inva- hematoma (esp. with epidural catheters,
sive surgical procedures. May restart as spinal trauma) were reported. Discon-
soon as adequate hemostasis is achieved, tinuation in the absence of other adequate
noting that the time of onset of pharma- anticoagulants may increase the risk of
codynamic effect is 1–2 hrs. ischemic events, stroke. May increase risk
of epidural or spinal hematomas, which can
Transition Guideline to Edoxaban lead to long-term or permanent paralysis.
From warfarin or other vitamin K Protamine sulfate, vitamin K, tranexamic
antagonists: Discontinue warfarin and acid are not expected to reverse antico-
start edoxaban when INR is less than or agulant effect. Interstitial lung disease was
equal to 2.5. From oral anticoagu- reported in less than 1% of pts.
lants other than warfarin or other
vitamin K antagonists: Discontinue NURSING CONSIDERATIONS
current oral anticoagulant and start
edoxaban at the time of the next sched- BASELINE ASSESSMENT
uled dose of the other oral anticoagulant. Obtain baseline renal function test, esp.
From LMWH: Discontinue LMWH and creatinine clearance; PT/INR in pts tran-
Canadian trade name Non-Crushable Drug High Alert drug
392 efavirenz/lamivudine/tenofovir
sitioning on or off warfarin therapy. Do HBV following discontinuation. If
not initiate if CrCl greater than 95 mL/min. discontinuation occurs, monitor
Question history of bleeding d­isorders, hepatic function for at least several
mos. Initiate anti-HBV therapy if
recent surgery, spinal procedures, in- warranted.
tracranial hemorrhage, bleeding ulcers, Do not confuse efavirenz/lami-
open wounds, anemia, renal/hepatic im- vudine/tenofovir (Symfi Lo) with
pairment, trauma. Receive full medication abacavir/dolutegravir/lamivu-
E history including herbal products. dine (Triumeq), abacavir/lami-
INTERVENTION/EVALUATION vudine/zidovudine (Trizivir),
bictegravir/emtricitabine/
Monitor renal function test; occult urine/
tenofovir (Biktarvy), efavirenz/
stool, urine output. Monitor for symp-
emtricitabine/tenofovir (Atri-
toms of hemorrhage: abdominal/back
pla), or emtricitabine/lopinavir/
pain, headache, altered mental status,
ritonavir/tenofovir (Kaletra).
weakness, paresthesia, aphasia, vision
changes, GI bleeding. Question for in- FIXED-COMBINATION(S)
crease in menstrual bleeding/discharge.
Symfi: efavirenz/lamivudine/tenofovir
Assess peripheral pulses; skin for ecchy-
(antiretrovirals).
mosis, petechiae. Assess urine output for
hematuria. uCLASSIFICATION
PATIENT/FAMILY TEACHING PHARMACOTHERAPEUTIC: Non-
• Do not discontinue current blood thin- nucleoside reverse transcriptase
ning regimen or take any newly prescribed inhibitor, nucleoside reverse tran-
medication unless approved by physician scriptase inhibitor, nucleotide re-
who started anticoagulant therapy. • Sud- verse transcriptase inhibitor. CLINI-
denly stopping therapy may increase risk of CAL: Antiretroviral agent (anti-HIV).
stroke or blood clots. Refill prescriptions
so that next scheduled dose is not USES
missed. • Immediately report bleeding of
any kind. • Avoid alcohol, aspirin, Treatment of HIV-1 infection in adults
NSAIDs. • Consult physician before sur- and pediatric pts weighing at least 40 kg
gery/dental work. • Use electric razor, (Symfi) or 35 kg (Symfi Lo).
soft toothbrush to prevent bleeding. • Re- PRECAUTIONS
port any numbness, muscular weakness,
signs of stroke (confusion, headache, one- Contraindications: Hypersensitivity to
sided weakness, trouble speaking), bloody efavirenz, lamivudine, tenofovir. History
stool or urine, nosebleeds. • Monitor of toxic skin reactions (e.g., erythema
changes in urine output. multiforme, Stevens-Johnson syndrome,
toxic skin eruptions). Concomitant use
of elbasvir, grazoprevir. Cautions: Renal/
hepatic impairment, hyperlipidemia,
efavirenz/lamivudine/ psychiatric illness (e.g., depression,
tenofovir psychosis, suicidal ideation); history
of pathological fracture, osteoporosis,
e-fav-ir-enz/la-miv-ue-deen/ten-oh- osteopenia; seizure disorder. Not rec-
foe-veer ommended in pts with CrCl less than 50
(Symfi, Symfi Lo) mL/min, end-stage renal disease requir-
j BLACK BOX ALERT jSevere ing dialysis, moderate to severe hepatic
exacerbations of hepatitis B impairment. History of pancreatitis
virus (HBV) infection reported (pediatric pts).
in pts coinfected with HIV-1 and

underlined – top prescribed drug


efavirenz/lamivudine/tenofovir 393

ACTION may decrease concentration/effect. May


Efavirenz (non-nucleoside reverse decrease concentration/effect of itra-
transcriptase inhibitor) blocks RNA- conazole, ketoconazole. Opioid
dependent and DNA-dependent DNA agonists (e.g., morphine, oxyCO-
polymerase activities. Lamivudine DONE) may increase CNS depression.
(nucleoside reverse transcriptase inhibi- HERBAL: Ginkgo biloba, St. John’s
tor) inhibits HIV reverse transcription via wort may decrease concentration/effect.
viral DNA chain termination. Tenofovir Herbals with sedative properties E
(nucleotide reverse transcriptase inhibi- (e.g., chamomile, kava kava, vale-
tor) interferes with the HIV RNA-depen- rian) may increase CNS depression.
dent DNA polymerase. Therapeutic FOOD: High-fat meals increase efavirenz
Effect: Interferes with HIV replication. absorption, increasing CNS effects. LAB
VALUES: May increase serum ALT/AST, bil-
PHARMACOKINETICS irubin, creatine kinase (CK), cholesterol,
Widely distributed. Efavirenz metabolized triglycerides. May decrease neutrophils.
in liver. Tenofovir metabolized by enzymatic
AVAILABILITY (Rx)
hydrolysis, mediated by macrophages and
hepatocytes. Protein binding: (efavirenz): Fixed-Dose Combination Tablets: (efavi-
greater than 99%; (lamivudine): less than renz/lamivudine/tenofovir [DF]): Symfi:
36%, (tenofovir): less than 1%. Peak plasma 600 mg/300 mg/300 mg; Symfi Lo: 400
concentration: (efavirenz): 3–5 hrs. Efavi- mg/300 mg/300 mg.
renz excreted in feces (61%), urine (34%).
ADMINISTRATION/HANDLING
Lamivudine excreted primarily in urine.
Tenofovir excreted primarily in urine (70– PO
80%). Half-life: (efavirenz): 52–76 hrs; • Administer on an empty stomach.
(lamivudine): 5–7 hrs; (tenofovir): 17 hrs. • To improve the tolerability of nervous sys-
tem symptoms, give preferably at bedtime.
LIFESPAN CONSIDERATIONS
INDICATIONS/ROUTES/DOSAGE
Pregnancy/Lactation: Avoid preg-
nancy, may cause fetal harm. Females of HIV Infection
reproductive potential must use effective PO: ADULTS, CHILDREN WEIGHING GREATER
contraceptive during treatment and up THAN 35 KG: 1 tablet once daily at bedtime.
to 12 wks after discontinuation. Breast- Dosage in Renal Impairment
feeding not recommended due to risk of CrCl greater than 50 mL/min: No
postnatal HIV transmission. Efavirenz/ dose adjustment. CrCl less than 50
lamivudine/tenofovir is secreted in breast mL/min, ESRD requiring HD: Not
milk. Children: Safety and efficacy not recommended.
established in children weighing less than
35 kg. May have increased risk of pan- Dosage in Hepatic Impairment
creatitis. Elderly: May have increased Mild impairment: No dose adjustment.
risk of adverse reactions/toxic reactions. Moderate to severe impairment: Not
recommended.
INTERACTIONS
DRUG: May decrease concentra- SIDE EFFECTS
tion/effects of axitinib, bosutinib, Occasional (18%–5%): Rash, pruritus,
cobimetinib, dasabuvir, ketocon- urticaria, headache, pain, diarrhea,
azole, neratinib, olaparib, rano- depression, nausea, fever, abdominal pain,
lazine, sonidegib, velpatasvir. Car back pain, asthenia, vomiting, insomnia,
BAMazepine may decrease effect of efa- arthralgia. Rare (4%–1%): Dyspepsia, diz-
virenz. Strong CYP3A4 inducers (e.g., ziness, myalgia, peripheral neuropathy,
carBAMazepine, phenytoin, rifAMPin) peripheral neuritis, neuropathy.
Canadian trade name Non-Crushable Drug High Alert drug
394 efavirenz/lamivudine/tenofovir

ADVERSE EFFECTS/TOXIC screen for contraindications/interactions.


REACTIONS Concomitant use of other medications may
May cause new or worsening renal failure need to be adjusted. Question possibility of
including Fanconi syndrome (renal tubular pregnancy. Question history of hepatic/renal
injury, nonabsorption of essential electro- impairment, hyperlipidemia, hypersensitiv-
lytes, acids, buffers in renal tubules). Renal ity reactions, decreased mineral bone den-
tubular injury may lead to rhabdomyolysis, sity, osteopenia, psychiatric illness, seizure
E osteomalacia, muscle weakness, myopathy. disorder; pancreatitis (in children). Verify
May decrease bone mineral density, lead- use of effective contraception in females of
ing to pathological fractures. May cause reproductive potential. Question plans of
redistribution/accumulation of body fat breastfeeding. Offer emotional support.
(lipodystrophy). Fatal cases of lactic aci- INTERVENTION/EVALUATION
dosis, severe hepatomegaly with steatosis
Monitor CD4+ count, viral load, HIV-1
(fatty liver) were reported. Fatal cases
RNA level for treatment effectiveness.
of hepatitis, fulminant hepatitis, hepatic
Monitor LFT; assess for hepatic injury
injury requiring liver transplantation were
(bruising, hematuria, jaundice, right up-
reported. If therapy is discontinued, pts
per abdominal pain, nausea, vomiting,
coinfected with hepatitis B or C virus have
weight loss). If discontinuation of drug
an increased risk for viral replication,
regimen occurs, monitor hepatic function
worsening of hepatic function, and may
for at least several months. Initiate anti-
experience hepatic decompensation and/
HBV therapy if warranted. Obtain serum
or failure. Suicidal ideation, depression,
lactate level if lactic acidosis suspected.
suicide attempt reported in less than 1%
Monitor renal function as clinically in-
of pts (primarily occurred in pts with prior
dicated. An increase in serum creatinine
psychiatric illness). May induce immune
greater than 0.4 mg/dL from baseline
recovery syndrome (inflammatory response
may indicate renal impairment. If other
to dormant opportunistic infections such as
concomitant medications were not dis-
Mycobacterium avium, cytomegalovirus,
continued or adjusted, closely monitor
PCP, tuberculosis or acceleration of autoim-
for adverse effects/toxic reactions. Moni-
mune disorders including Graves’ disease,
tor for immune recovery syndrome, esp.
polymyositis, Guillain-Barré). CTCAE Grade
after initiating treatment. Cough, dyspnea,
4 rash, Stevens-Johnson syndrome, toxic
fever, excess band cells on CBC may in-
skin eruptions occurred in less than 1% of
dicate acute infection (WBC may be un-
pts. Seizure activity, QTc interval prolonga-
reliable in pts with uncontrolled HIV in-
tion were reported in pts taking efavirenz
fection). Monitor daily pattern of bowel
products. Infections including pneumonia
activity, stool consistency; I&Os. Monitor
(5% of pts), herpes zoster (3% of pts) were
for seizure activity, esp. in pts with seizure
reported.
disorder. Assess skin for toxic skin reac-
tions, rash. Screen for psychiatric symp-
NURSING CONSIDERATIONS toms (agitation, delusions, depression,
BASELINE ASSESSMENT paranoia, psychosis, suicidal ideation).
Obtain serum amylase, lipase level if acute
Obtain LFT, BUN, serum creatinine, CrCl,
pancreatitis suspected in children.
eGFR, CD4+ count, viral load, HIV-1 RNA
level; urine glucose, urine protein, preg- PATIENT/FAMILY TEACHING
nancy test in females of reproductive po- • Treatment does not cure HIV infection
tential. Obtain serum phosphate level in or reduce risk of transmission. Practice
pts with renal impairment. Test all pts for safe sex with barrier methods or absti-
HBV infection. Receive full medication nence. • Take on an empty stomach,
history (including herbal products) and preferably at bedtime (may help with

underlined – top prescribed drug


elbasvir/grazoprevir 395
nervous system symptoms). • Drug re- USES
sistance can form if treatment is inter- Treatment of chronic hepatitis C virus
rupted; do not run out of supply. • As genotypes 1 or 4 infection in adults, with
immune system strengthens, it may re- or without ribavirin.
spond to dormant infections hidden
within the body. Report any new fever, PRECAUTIONS
chills, body aches, cough, night sweats, Contraindications: Hypersensitivity to
shortness of breath. • Fatal cases of elbasvir or grazoprevir, decompensated E
liver inflammation or failure have oc- hepatic cirrhosis, moderate or severe
curred; report abdominal pain, clay-col- hepatic impairment; concomitant use of
ored stools, yellowing of skin or eyes, organic anion transporting polypeptides
weight loss. • Report symptoms of kid- 1B1/3 (OATP1B1/3) inhibitors, strong
ney inflammation or disease (decreased CYP3A inducers. Concomitant use of ata-
urine output, abdominal pain, darkened zanavir, carBAMazepine, cycloSPORINE,
urine); toxic skin reactions (rash, pus- darunavir, efavirenz, lopinavir, phe-
tules, skin eruptions); seizure activity or nytoin, rifAMPin, saquinavir, St. John’s
convulsions. • Pancreatitis can occur wort, tipranavir. Any contraindications or
in children; report any new or worsening hypersensitivity to ribavirin (if used with
abdominal pain that radiates to the back treatment regimen). Cautions: HIV infec-
or shoulder, with or without nausea/ tion, mild hepatic impairment. Safety and
vomiting. • Lactating females should efficacy not established in pts with hepa-
not breastfeed. Females of reproductive titis B virus coinfection, liver transplant
potential must use effective contraceptive recipients.
during treatment and up to 12 wks after
last dose. • Decreased bone density ACTION
may lead to pathological fractures; report Elbasvir inhibits hepatitis C virus (HCV)
bone/extremity pain, suspected frac- NS5A protein, which is essential for
tures. • Antiretrovirals may cause ex- viral RNA replication and virion assem-
cess body fat in upper back, neck, breast, bly. Grazoprevir inhibits HCV NS3/4A
trunk, while also causing decreased body protease needed for processing HCV-
fat in legs, arms, face. • Do not take encoded polyproteins, which is essen-
newly prescribed medications, including tial for viral replication. Therapeutic
OTC drugs, unless approved by doctor Effect: Inhibits viral replication of
who originally started treatment. hepatitis C virus.
PHARMACOKINETICS
Widely distributed. Metabolized in liver.
elbasvir/grazoprevir Protein binding: elbasvir (99.9%),
grazoprevir (98.8%). Peak plasma con-
el-bas-vir/graz-oh-pre-vir centration: 3 hrs. Steady state reached in
(Zepatier) approx. 6 days. Excreted in feces (greater
Do not confuse elbasvir with than 90%), urine (less than 1%). Half-
daclatasvir, ombitasvir or life: elbasvir: 24 hrs; grazoprevir:
grazoprevir with boceprevir or 31 hrs.
simeprevir.
LIFESPAN CONSIDERATIONS
uCLASSIFICATION
Pregnancy/Lactation: Use caution
PHARMACOTHERAPEUTIC: NS5A in pregnancy. Unknown if distributed
inhibitor/protease inhibitor. CLINI- in breast milk. When used with riba-
CAL: Antihepaciviral. virin, breastfeeding and pregnancy
are contraindicated during treatment
Canadian trade name Non-Crushable Drug High Alert drug
396 elbasvir/grazoprevir
and up to 6 mos after discontinua- Treatment Regimen and Duration
tion. Children: Safety and efficacy PO: ADULTS, ELDERLY: Genotype 1a:
not established. Elderly: May have Treatment-naïve or peginterferon
increased risk of hepatotoxicity. alfa (PegIFN)/ribavirin (RBV)–expe-
rienced without baseline NS5A poly-
INTERACTIONS morphisms: 1 tablet once daily for 12
DRUG: Anticonvulsants (e.g., car- wks. Genotype 1a: Treatment-naïve
E BAMazepine, phenytoin), anti- or PegIFN/RBV–experienced with
mycobacterials (e.g., rifabutin, baseline NS5A polymorphisms: 1
rifAMPin), efavirenz may signifi- tablet once daily with ribavirin for 16
cantly decrease concentration/effect; wks. Genotype 1b: Treatment-naïve
use contraindicated. Atazanavir, or PegIFV/RBV–experienced: 1 tab-
darunavir, cycloSPORINE may sig- let once daily for 12 wks. Genotype 1a
nificantly increase risk of hepatotox- or 1b: PegIFV/RBV/protease inhibi-
icity; use contraindicated. Moderate tor–experienced: 1 tablet once daily
CYP3A inducers (e.g., amiodarone, with ribavirin for 12 wks. Genotype 4:
dilTIAZem, fluconazole) may Treatment-naïve: 1 tablet once daily
decrease concentration/effect. Elvite- for 12 wks. Genotype 4: PegIFN/RBV–
gravir/cobicistat/emtricitabine/ experienced: 1 tablet once daily with
tenofovir (disoproxil or alafen- ribavirin for 16 wks.
amide), ketoconazole may increase
Treatment-Induced Hepatotoxicity
concentration/effect. May increase
concentration/effect of atorvastatin, Consider discontinuation in pts with per-
fluvastatin, HYDROcodone, lovas- sistent serum ALT elevation greater than 10
tatin, niMODipine, rosuvastatin, times upper limit of normal (ULN). Perma-
simvastatin, tacrolimus. Acetamin- nently discontinue if serum ALT elevation is
ophen may increase risk of hepato- accompanied with elevated alkaline phos-
toxicity. HERBAL: St. John’s wort may phatase, conjugated bilirubin, prolonged
decrease concentration/effect; use INR, or signs of acute hepatic inflammation.
contraindicated. FOOD: None known. Dosage in Renal Impairment
LAB VALUES: May decrease Hgb. May No dose adjustment.
increase serum ALT, bilirubin.
Dosage in Hepatic Impairment
AVAILABILITY (Rx) Mild impairment: No dose adjust-
Fixed-Dose Combination Tablets: elbasvir ment. Moderate to severe impair-
50 mg/grazoprevir 100 mg. ment: Contraindicated.

ADMINISTRATION/HANDLING SIDE EFFECTS


PO Occasional (11%–3%): Fatigue, headache,
• Give without regard to food. diarrhea, nausea, insomnia, dyspnea, rash,
pruritus, irritability. Rare (2%): Abdominal
INDICATIONS/ROUTES/DOSAGE pain, arthralgia.
Note: NS5A resistance testing recom-
mended in HCV genotype 1a infected ADVERSE EFFECTS/TOXIC
pts prior to initiating treatment with REACTIONS
Zepatier. Serum ALT elevation up to 5 times ULN
reported in 1% of pts. Serum bilirubin
Chronic Hepatitis C Virus Infection elevation greater than 2.5 times ULN
PO: ADULTS, ELDERLY: 1 tablet once daily occurred in 6% of pts. Serum ALT elevation
(with or without ribavirin). occurred more frequently in the elderly,
female pts, and pts of Asian ancestry.

underlined – top prescribed drug


eletriptan 397

NURSING CONSIDERATIONS eletriptan


BASELINE ASSESSMENT
Obtain CBC, LFT, HCV-RNA level; preg- el-e-trip-tan
nancy test in female pts of reproductive (Relpax)
potential. Confirm hepatitis C genotype. uCLASSIFICATION
In pts with HCV genotype 1a, recom-
mend testing for the presence of NS5A PHARMACOTHERAPEUTIC: Seroto- E
resistance-associated polymorphisms nin receptor agonist. CLINICAL: An-
prior to initiation. Receive full medica- timigraine.
tion history including herbal products;
screen for contraindications. Question USES
history of chronic anemia, hepatitis
B virus infection, HIV infection, liver Treatment of acute migraine headache
transplantation. with or without aura.

INTERVENTION/EVALUATION PRECAUTIONS
Obtain LFT at wk 8, then as clinically Contraindications: Hypersensitivity to
indicated. For pts receiving 16 wks of eletriptan. Arrhythmias associated with
therapy, obtain additional LFT at wk 12. conduction disorders, cerebrovascular
Monitor CBC periodically; HCV-RNA lev- syndrome including strokes and transient
els at wks 4, 8, 12, 16 and as clinically ischemic attacks (TIAs), coronary artery
indicated. Monitor for hepatotoxicity. disease, hemiplegic or basilar migraine,
Assess for anemia-related dizziness, ischemic heart disease, peripheral vas-
exertional dyspnea, fatigue, weakness, cular disease including ischemic bowel
syncope. Encourage nutritional intake. disease, severe hepatic impairment,
Assess for decreased appetite, weight uncontrolled hypertension; use within
loss. Obtain monthly pregnancy tests 24 hrs of treatment with another 5-HT1
in females of reproductive potential if agonist, an ergotamine-containing or
treated with ribavirin. ergot-type medication such as dihydroer-
gotamine (DHE) or methysergide. Recent
PATIENT/FAMILY TEACHING use (within 72 hrs) of strong CYP3A4
• Blood levels will be drawn rou- inhibitors (e.g., clarithromycin, keto-
tinely. • Treatment may be used in conazole, itraconazole, ritonavir). Cau-
combination with ribavirin (inform pt of tions: Mild to moderate renal/hepatic
side effects/toxic reactions). If therapy impairment, controlled hypertension,
includes ribavirin, female pts of repro- history of CVA.
ductive potential should avoid pregnancy
during treatment and up to 6 mos after ACTION
last dose. • Do not take newly pre- Selective agonist for serotonin in cranial
scribed medication unless approved by arteries; causes vasoconstriction and
the doctor who originally started treat- reduces inflammation. Therapeutic
ment. • Do not take herbal products, Effect: Relieves migraine headache.
esp. St. John’s wort. • Avoid alcohol,
grapefruit products. • Report signs of PHARMACOKINETICS
treatment-induced liver injury such as Well absorbed after PO administra-
abdominal pain, clay-colored stool, dark tion. Metabolized by liver. Excreted in
amber urine, decreased appetite, fatigue, urine. Half-life: 4.4 hrs (increased
weakness, yellowing of the skin or in hepatic impairment, elderly [older
eyes. • Maintain proper nutritional in- than 65 yrs]).
take.

Canadian trade name Non-Crushable Drug High Alert drug


398 elotuzumab

LIFESPAN CONSIDERATIONS CVA) occur rarely, particularly in pts with


Pregnancy/Lactation: May decrease hypertension, obesity, diabetes, strong
possibility of ovulation. Distributed in family history of coronary artery dis-
breast milk. Children: Safety and efficacy ease; smokers; males older than 40 yrs;
not established. Elderly: Increased risk postmenopausal women. May cause GI
of hypertension in those older than 65 yrs. ischemia, bowel infarction, non–cardiac-
related vasospasms including peripheral
E INTERACTIONS vascular ischemia, Raynaud’s syndrome.
DRUG: Ergot derivatives (e.g., ergot- Overuse may increase frequency, occur-
amine) may increase vasoconstrictive rence of headaches.
effect. Strong CYP3A4 inhibitors NURSING CONSIDERATIONS
(e.g., clarithromycin, ketoconazole,
ritonavir) may increase concentration/ BASELINE ASSESSMENT
effect. MAOIs (e.g., phenelzine, sele- Question pt regarding onset, location,
giline) may cause serotonin syndrome. duration of migraine, possible precipitat-
HERBAL: None significant. FOOD: None ing symptoms. Obtain baseline B/P for
known. LAB VALUES: None significant. evidence of uncontrolled hypertension
(contraindication).
AVAILABILITY (Rx)
INTERVENTION/EVALUATION
Tablets: 20 mg, 40 mg.
Assess for relief of migraine headache,
ADMINISTRATION/HANDLING potential for photophobia, phonopho-
PO bia (sound sensitivity), nausea, vomit-
• Give without regard to food. • Do ing. Monitor for cardiac arrhythmia,
not break, crush, dissolve, or divide film- coronary events, hypertension, hypersen-
coated tablets. sitivity reaction.
PATIENT/FAMILY TEACHING
INDICATIONS/ROUTES/DOSAGE
• Take a single dose as soon as symp-
Acute Migraine Headache
toms of an actual migraine attack ap-
PO: ADULTS, ELDERLY: Initially, 20–40
pear. • Medication is intended to re-
mg as a single dose. Maximum: 40 mg.
lieve migraine headaches, not to prevent
If headache improves but then returns,
or reduce number of attacks. • Avoid
dose may be repeated after 2 hrs. Maxi-
tasks that require alertness, motor skills
mum: 80 mg/day.
until response to drug is estab-
Dosage in Renal/Hepatic Impairment lished. • Immediately report palpita-
No dose adjustment. Not recommended tions, pain/tightness in chest/throat, sud-
in severe hepatic impairment. den or severe abdominal pain, pain/
weakness of extremities.
SIDE EFFECTS
Occasional (6%–5%): Dizziness, drowsi-
ness, asthenia, nausea. Rare (3%–2%): Par-
esthesia, headache, dry mouth, warm or hot elotuzumab
sensation, dyspepsia, dysphagia.
el-oh-tooz-ue-mab
ADVERSE EFFECTS/TOXIC (Empliciti)
REACTIONS Do not confuse elotuzumab
Cardiac reactions (ischemia, coronary with alemtuzumab, eculizumab,
artery vasospasm, MI), noncardiac vaso- evolocumab, pertuzumab, gem-
spasm-related reactions (hemorrhage, tuzumab, trastuzumab.

underlined – top prescribed drug


elotuzumab 399
uCLASSIFICATION LIFESPAN CONSIDERATIONS
PHARMACOTHERAPEUTIC: Anti- Pregnancy/Lactation: Avoid preg-
SLAMF7. Monoclonal antibody. CLIN- nancy; may cause fetal harm/malfor-
ICAL: Antineoplastic. mations/fetal demise when used with
lenalidomide. Unknown if distributed in
breast milk. However, immunoglobulin G
USES (IgG) is present in breast milk. Breast-
Treatment of multiple myeloma (in feeding contraindicated when used with E
combination with lenalidomide and concomitant lenalidomide treatment.
dexamethasone) in pts who have Men: Lenalidomide is present in semen.
received one to three prior therapies Recommend use of barrier methods dur-
or (in combination with pomalidomide ing sexual activity. Children: Safety and
and dexamethasone) in pts who have efficacy not established. Elderly: No
received at least two prior therapies age-related precautions noted.
including lenalidomide and a protea-
some inhibitor. INTERACTIONS
DRUG: May increase immunosuppres-
PRECAUTIONS sant/toxic effects of immunosuppres-
Contraindications: Hypersensitivity to sants (e.g., fingolimod, leflunomide,
elotuzumab. Cautions: Diabetes, base- nivolumab). Roflumilast may increase
line cytopenias, hypertension; history immunosuppressant effect. May enhance
of chronic opportunistic infections adverse/toxic effect of live vaccines; may
(esp. viral infections, fungal infections), decrease therapeutic effect of vaccines.
conditions predisposing to infection HERBAL: Echinacea may decrease effect.
(e.g., diabetes, kidney failure, open FOOD: None known. LAB VALUES: May
wounds). Concomitant use of medica- be detected on both serum protein electro-
tions known to cause bradycardia (e.g., phoresis and immunofixation assays used
antiarrhythmics, beta blockers, calcium to monitor multiple myeloma endogenous
channel blockers). Concomitant use of M-protein. May affect the determination of
live vaccines not recommended during complete response and disease progres-
treatment and up to 3 mos after discon- sion of some pts with IgG kappa myeloma
tinuation. Avoid use during severe active protein. Expected to decrease lympho-
infection. cytes, leukocytes, platelets. May decrease
serum albumin, bicarbonate, calcium.
ACTION May increase serum alkaline phosphatase,
Binds to and specifically targets signal- ALT, AST, glucose, potassium.
ing lymphocytic activation molecule
family member 7 (SLAMF7), a protein AVAILABILITY (Rx)
that is expressed on most myeloma Injection, Powder for Reconstitution: 300
and natural killer cells. Directly acti- mg, 400 mg.
vates natural killer cells and facili-
tates cellular death. Therapeutic ADMINISTRATION/HANDLING
Effect: Inhibits tumor cell growth IV
and metastasis.
Reconstitution • Calculate the dose
PHARMACOKINETICS and number of vials required based on
Widely distributed. Metabolism not speci- weight in kg. • Reconstitute the 300-mg
fied. Elimination not specified. Half- vial with 13 mL of Sterile Water for Injection
life: Not specified; 97% of steady-state or the 400-mg vial with 17 mL of Sterile
concentration is expected to be elimi- Water for Injection using an 18-g or lower
nated within 82 days. (e.g., 17, 16, or 15) needle. • Gently roll
Canadian trade name Non-Crushable Drug High Alert drug
400 elotuzumab
vial upright to mix. To dissolve any powder Storage • Refrigerate intact vials until
left on top of vial or stopper, gently invert time of use. • Do not freeze or
vial several times. • Do not shake or agi- shake. • Refrigerate diluted solution up
tate. • The powder should dissolve in less to 24 hrs. • May store at room tem-
than 10 mins. • After dissolution, allow perature up to 8 hrs (of the total 24
vials to stand for 5–10 mins. • Visually hrs). • Diluted solution must be ad-
inspect solution for particulate matter of ministered within 24 hrs of reconstitu-
E discoloration. Solution should appear tion. • Protect from light.
clear, colorless to slightly yellow. Discard if
solution is cloudy or discolored or if for- IV INCOMPATIBILITIES
eign particles are observed. Each vial con- Do not mix with other medications.
tains an overfill volume to allow for a spe-
cific withdrawal of 12 mL (300-mg vial) or INDICATIONS/ROUTES/DOSAGE
16 mL (400-mg vial). • Final concentra- Multiple Myeloma
tion of withdrawn volume (without overfill) Note: Premedicate with dexamethasone,
will equal 25 mg/mL. • Dilute in 230 mL H1 or H2 blocker, and acetaminophen
of 0.9% NaCl or 5% Dextrose injection in 45–90 min before infusion.
polyvinyl chloride or polyolefin infusion IV: ADULTS, ELDERLY: (In combination
bag. • Mix by gentle inversion; do not with lenalidomide and dexametha-
shake or agitate. • The volume may be sone): Cycles 1 and 2: 10 mg/kg once
adjusted in order to not exceed 5 mL/kg of wkly on days 1, 8, 15, 22 of 28-day cycle.
pt weight at any given dose. Cycles 3 and beyond: 10 mg/kg once
Infusion guidelines • Prior to admin- q2wks on days 1 and 15 of 28-day cycle.
istration, premedicate with dexametha- Continue until disease progression or unac-
sone, acetaminophen, antihistamine (H1 ceptable toxicity. (In combination with
antagonist, plus H2 antagonist) approx. pomalidomide and dexamethasone):
45–90 mins before each infusion (see Cycles 1 and 2: 10 mg/kg once wkly on
manufacturer guidelines). • Use an in- days 1, 8, 15, 22 of 28-day cycle. Cycles
line, sterile, nonpyrogenic, low protein- 3 and beyond: 20 mg/kg once q4wks on
binding filter (0.2–1.2 mm). • Infuse via day 1 of 28-day cycle. Continue until disease
dedicated line using an infusion pump. progression or unacceptable toxicity.
Rate of administration • First infu-
sion (cycle 1, dose 1): Infuse at 0.5 mL/ Dose Modification
min for the first 30 mins. If no infusion Infusion Reactions
reactions occur, may increase to 1 mL/min Grade 2 or higher reaction: Interrupt
for next 30 mins. If tolerated, may increase infusion until symptoms improve. Once
to 2 mL/min. Maximum rate: 2 mL/ resolved to Grade 1 or 0, resume infusion
min. • Second infusion (cycle 1, at 0.5 mL/min. If tolerated, increase in
dose 2): Initiate at 1 mL/min for first 30 increments of 0.5 mL/min q30mins back
mins if no infusion reactions occurred to previous rate. May further increase
during first infusion. If tolerated, may in- rate as indicated if no reaction recurs.
crease to 2 mL/min until infusion com- If infusion reaction recurs, stop infusion
pleted. Maximum rate: 2 mL/ and do not restart for that day.
min. • Subsequent infusions (cycle Dosage in Renal/Hepatic Impairment
1, doses 3 and 4, all subsequent infu- Not specified; use caution.
sions): Initiate at 2 mL/min until comple-
tion if no infusion reactions occurred dur- SIDE EFFECTS
ing prior infusion. Maximum rate: 2 mL/ Frequent (61%–20%): Fatigue, diarrhea,
min. In pts who have received four cycles pyrexia, constipation, cough, periph-
of treatment, infusion rate may be in- eral neuropathy, decreased appetite.
creased to maximum rate of 5 mL/min.

underlined – top prescribed drug


elotuzumab 401
Occasional (16%–10%): Extremity pain, known to cause bradycardia, hypergly-
headache, vomiting, decreased weight, cemia. Screen for active infection. Offer
oropharyngeal pain, hypoesthesia, mood emotional support.
change, night sweats.
INTERVENTION/EVALUATION
ADVERSE EFFECTS/TOXIC Obtain CBC, BMP, LFT, ionized calcium
REACTIONS periodically. Administer in an environ-
All cases were reported in combination ment equipped to monitor for and man- E
with lenalidomide and dexamethasone. age infusion reactions. If infusion reaction
Infusion reactions reported in 10% of pts. of any grade/severity occurs, immediately
Most infusion reactions were Grade 3 and interrupt infusion and manage symptoms.
lower. Lymphopenia, leukopenia, throm- Accurately record characteristics of infu-
bocytopenia are expected responses to sion reactions (severity, type, time of on-
therapy. Infections were reported in 81% set). Infusion reactions may affect future
of pts. Grade 3 or 4 infections occurred infusion rates. Monitor HR, BP q30mins
in 28% of pts. Nasopharyngitis (25% of during infusion and for at least 2 hrs after
pts), upper respiratory tract infection completion in pts with prior hemodynamic
(23% of pts), opportunistic infection reactions. Cough, dyspnea, hypoxia, tachy-
(22% of pts), herpes zoster (14% of cardia may indicate pulmonary embolism.
pts), fungal infection (10% of pts), influ- Monitor for bradycardia, cataracts, hyper-
enza; second primary malignancies, skin glycemia, hyperkalemia, hypersensitiv-
malignancies, solid tumors, malignant ity reaction, hepatotoxicity, neuropathy,
neoplasms; tachycardia, bradycardia, tachycardia. Assess for new primary ma-
systolic or diastolic hypertension, hypo- lignancies (solid tumors, skin cancers);
tension; pulmonary embolism may occur. skin for new lesions, moles. Monitor
Hepatotoxicity with elevation of serum daily pattern bowel activity, stool consis-
alkaline phosphatase greater than 2 times tency. Obtain urine, serum pregnancy test
upper limit of normal (ULN), serum ALT/ periodically throughout therapy.
AST greater than 3 times ULN, total bili- PATIENT/FAMILY TEACHING
rubin greater than 2 times ULN reported
in 3% of pts. Other adverse effects may • Blood levels, ECGs will be monitored
include cataracts (12% of pts), hyper- routinely. • Treatment may depress your
glycemia (89% of pts), hypersensitivity immune system and reduce your ability to
reaction (greater than 5% of pts). Immu- fight infection. Report symptoms of infec-
nogenicity (auto-elotuzumab antibodies) tion such as body aches, chills, cough, fa-
occurred in 19% of pts. Thrombocytope- tigue, fever. Avoid those with active infec-
nia may increase risk of bleeding. tion. • Therapy may decrease your heart
rate, esp. in those taking medications that
NURSING CONSIDERATIONS lower heart rate; report dizziness, chest
pain, palpitations, or fainting. • Avoid
BASELINE ASSESSMENT pregnancy. Do not breastfeed. • Male
Obtain CBC, BMP, LFT; serum ionized cal- pts should use condoms during sexual
cium; capillary blood glucose, vital signs; activity. • Treatment includes a steroid
pregnancy test in female pts of reproduc- that may raise blood sugar levels; report
tive potential. Obtain baseline ECG in pts dehydration, blurry vision, confusion, fre-
concurrently using medications known quent urination, increased thirst, fruity
to cause bradycardia. Question history breath. • Report allergic reactions of
of chronic opportunistic infections, dia- any kind. • Abdominal pain, easy bruis-
betes, hepatic impairment, pulmonary ing, clay-colored stools, dark-amber
embolism; prior infusion or hypersensi- urine, fatigue, loss of appetite, yellowing of
tivity reactions. Screen for medications skin or eyes may indicate liver problem.

Canadian trade name Non-Crushable Drug High Alert drug


402 eltrombopag

ACTION
eltrombopag Binds to and activates human throm-
bopoietin (TPO) receptor. Activates
el-trom-boe-pag
intracellular signal pathways. Thera-
(Promacta, Revolade )
peutic Effect: Increases platelet count;
j BLACK BOX ALERT jMay increases proliferation and differentia-
cause hepatotoxicity. Measure
serum ALT, AST, bilirubin prior to tion of marrow progenitor cells.
E initiation of eltrombopag, every 2
wks during dose adjustment phase, PHARMACOKINETICS
and monthly following establish- Readily absorbed from gastrointestinal
ment of a stable dose. If bilirubin tract. Primarily distributed in blood cells.
is elevated, perform fractionation. Protein binding: 99%. Extensively metabo-
Discontinue if serum ALT levels
increase to 3 times or greater upper lized including oxidation, conjugation
limit of normal and are progres- with glucuronic acid or cysteine. Excreted
sive, persistent for 4 or more wks, ­primarily in feces. Half-life: 26–35 hrs.
accompanied by increased direct
bilirubin, clinical symptoms of he- LIFESPAN CONSIDERATIONS
patic injury, or evidence of hepatic Pregnancy/Lactation: Unknown if dis-
decompensation.
tributed in breast milk. Children: Safety
uCLASSIFICATION and efficacy not established. Elderly: Use
PHARMACOTHERAPEUTIC: Throm- caution due to increased frequency of
bopoietin receptor agonist. CLINI- hepatic, renal, cardiac dysfunction.
CAL: Hematopoietic, thrombopoietic. INTERACTIONS
DRUG: Aluminum, antacids, calcium,
USES iron, magnesium, sucralfate may
decrease concentration/effects. May increase
Treatment of thrombocytopenia in pts with concentration/effects of grazoprevir,
chronic immune (idiopathic) thrombo- topotecan, voxilaprevir. HERBAL: None
cytopenic purpura (ITP) with insufficient significant. FOOD: Dairy products may
response with corticosteroids, immunoglob- decrease concentration/effects. LAB VAL-
ulins, or splenectomy. Use only in pts who UES: May increase serum ALT, AST.
are at increased risk for bleeding; should
not be used to normalize platelet counts. AVAILABILITY (Rx)
Treatment of thrombocytopenia in pts with Tablets: 12.5 mg, 25 mg, 50 mg, 75 mg.
chronic hepatitis C virus infection to allow
the initiation and maintenance of interferon- ADMINISTRATION/HANDLING
based therapy. Treatment of severe (refrac- PO
tory) aplastic anemia in pts having an • Give on an empty stomach, either 1 hr
insufficient response to immunosuppressive before or 2 hrs after meal. • Give at
therapy. First-line treatment (in combination least 4 hrs before or 4 hrs after ingestion
with immunosuppressive therapy) of severe of antacids, food high in calcium or
aplastic anemia in pts 2 yrs and older. minerals, or calcium-fortified juices.
PRECAUTIONS INDICATIONS/ROUTES/DOSAGE
Contraindications:Hypersensitivity to Aplastic Anemia (Refractory)
eltrombopag. Cautions: Preexisting PO: ADULTS, ELDERLY: 50 mg once daily
hepatic impairment, renal impairment (25 mg for pts of East Asian ancestry
(any degree), myelodysplastic syndrome or hepatic impairment). Titrate dose
(may increase risk for hematologic based on platelet response. Adjust dose
malignancies). Pts with known risk for to maintain platelets more than 50,000/
thromboembolism, risk for cataracts. mm3. Maximum: 150 mg/day.
underlined – top prescribed drug
eltrombopag 403
First-Line Severe Aplastic Anemia Chronic Hepatitis C
PO: ADULTS, ELDERLY, CHILDREN 12 YRS No dose adjustment.
AND OLDER: 150 mg once daily (75 mg
once daily for pts of Asian ancestry) for Aplastic Anemia
6 mos. CHILDREN 6–11 YRS: 75 mg once Initial dose 25 mg once daily.
daily (37.5 mg once daily for pts of Asian
ancestry) for 6 mos. CHILDREN 2–5 YRS: SIDE EFFECTS
2.5 mg/kg (Maximum: 75 mg/dose) Frequent (6%–4%): Nausea, vomiting, E
once daily (1.25 mg/kg once daily for pts menorrhagia. Occasional (3%–2%): Myal-
of Asian ancestry. Maximum: 37.5 mg) gia, paresthesia, dyspepsia, ecchymosis,
for 6 mos. cataract, conjunctival hemorrhage.

ITP ADVERSE EFFECTS/TOXIC


PO: ADULTS, ELDERLY, CHILDREN 6 YRS REACTIONS
AND OLDER: Initially, 50 mg once daily May cause hepatotoxicity. Increases risk
(25 mg for pts of East Asian ancestry or of reticulin fiber deposits within bone
moderate to severe hepatic insufficiency marrow (may lead to bone marrow fibro-
or children 1 to 5 yrs of age). Then, sis). May produce hematologic malig-
adjust dose (25 mg to 75 mg once daily) nancies. May cause excessive increase in
to achieve and maintain platelet count of platelets, leading to thrombotic compli-
50,000 cells/mm3 or greater as neces- cations.
sary to reduce risk of bleeding. Maxi-
mum: 75 mg once daily. NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Chronic Hepatitis C–Associated
Thrombocytopenia Assess CBC and peripheral blood
PO: ADULTS, ELDERLY: Initially, 25 mg smears, LFT. Examine peripheral blood
once daily. Titrate dose based on platelet smear to establish extent of RBC and
response. Maximum: 100 mg once daily. WBC abnormalities. Conduct ocular
examination. Screen for hepatic/re-
Dosage Adjustment Based on Platelet nal impairment, myelodysplastic syn-
Response drome, history of thromboembolism.
Less than 50,000/ Increase by 25 mg Question use of antacids or herbal
mm3 (after at q2wks up to products.
least 2 wks) 100 mg/day
3 INTERVENTION/EVALUATION
200,000/mm or Decrease by 25 mg
more and 400,000/ Monitor CBC, platelet counts, periph-
mm3 or less eral blood smears, LFT throughout
More than 400,000/ Withhold; when less and following discontinuation. Moni-
mm3 than 150,000/mm3, tor for cataracts, hepatotoxicity during
resume with dose therapy.
reduced by 25 mg
More than 400,000/ Discontinue PATIENT/FAMILY TEACHING
3
mm after 2 wks
at lowest dose
• Lab values will be closely monitored
throughout therapy and for at least 4 wks
Dosage in Renal Impairment after last dose. • Report any yellowing
No dose adjustment. of the skin or eyes, unusual darkening of
the urine, unusual tiredness, pain in right
Dosage in Hepatic Impairment upper stomach area. • Do not take ant-
ITP acids, magnesium, or calcium products
Mild to severe Initial: 25 mg/day 4 hrs before or after dose. • Report
East Asian ancestry Initial: 12.5 mg/day changes in vision.

Canadian trade name Non-Crushable Drug High Alert drug


404 eluxadoline
and efficacy not established. Elderly: No
eluxadoline age-related precautions noted.
el-ux-ad-oh-leen INTERACTIONS
(Viberzi) DRUG: OATP1B1 inhibitors (e.g.,
cycloSPORINE, ritonavir, rifAMPin),
uCLASSIFICATION
gemfibrozil may increase concentration/
E PHARMACOTHERAPEUTIC: Mu- effect. Drugs that cause constipation
opioid receptor agonist. Schedule IV. (e.g., alosetron, anticholinergics
CLINICAL: GI agent. [e.g., diphenhydrAMINE], loper-
amide, opioids [e.g., morphine]) may
USES increase risk of serious constipation-
associated adverse effects. May increase
Treatment of irritable bowel syndrome
concentration of rosuvastatin, increas-
with diarrhea (IBS-D) in adults.
ing risk of myopathy/rhabdomyolysis.
PRECAUTIONS HERBAL: None significant. FOOD: High-
fat meals may decrease absorption. LAB
Contraindications: Hypersensitivity to
VALUES: May increase serum ALT, AST,
eluxadoline. Known or suspected bili-
lipase.
ary duct obstruction, sphincter of Oddi
disease or dysfunction; pts without a AVAILABILITY (Rx)
gallbladder; severe hepatic impair-
ment; severe constipation or sequelae Tablets: 75 mg, 100 mg.
from constipation, or known or sus-
pected mechanical GI obstruction.
ADMINISTRATION/HANDLING
History of alcoholism, alcohol abuse, PO
alcohol addiction, or consumption of • Administer with food. • If scheduled
more than 3 alcoholic beverages/day. dose is missed, give next dose at the
History of pancreatitis; structural dis- regular time; do not give 2 doses at once.
ease of the pancreas, including known
or suspected pancreatic duct obstruc-
INDICATIONS/ROUTES/DOSAGE
tion. Cautions: Mild to moderate hepatic Irritable Bowel Syndrome–Associated
impairment, respiratory disease. Diarrhea
PO: ADULTS, ELDERLY: 100 mg twice
ACTION daily. May decrease to 75 mg twice daily
Acts locally on mu opioid, delta opioid, if unable to tolerate 100-mg dose.
and kappa opioid receptors involved with
gut motility, pain sensations, and secre- Dose Modification
tion of liquids within the digestive tract. Pts who are unable to tolerate 100-mg
Therapeutic Effect: Reduces abdomi- dose, or are receiving concomitant
nal pain and diarrhea (without causing OATP1B1 inhibitors: 75 mg twice daily.
constipation). Pts who develop severe constipa-
tion for more than 4 days: Perma-
PHARMACOKINETICS nently discontinue.
Metabolism not specified. Protein binding: Dosage in Renal Impairment
81%. Peak plasma concentration: 1.5 hrs. Not specified; use caution.
Primarily excreted in feces (82%), urine
(less than 1%). Half-life: 3.7–6 hrs. Dosage in Hepatic Impairment
Mild to moderate impairment: 75
LIFESPAN CONSIDERATIONS
mg twice daily. Severe impairment:
Pregnancy/Lactation: Unknown if dis- Contraindicated.
tributed in breast milk. Children: Safety
underlined – top prescribed drug
elvitegravir/­cobicistat/­emtricitabine/­tenofovir 405

SIDE EFFECTS lipase level if acute pancreatitis, sphincter


Occasional (8%–4%): Constipation, nau- of Oddi spasm, biliary tract obstruction
sea, abdominal pain (upper or lower), suspected. Monitor for hypersensitivity re-
upper respiratory tract infection, vomit- action including dyspnea, rash, wheezing.
ing. Rare (3%–1%): Abdominal disten- Observe and record daily pattern of bowel
tion, dizziness, flatulence, rash, urticaria, activity, stool consistency. Encourage PO
fatigue, sedation, somnolence, euphoric intake. If an acute overdose occurs, a nar-
mood. cotic mu-opioid antagonist such as nalox- E
one may be considered if reversal of over-
ADVERSE EFFECTS/TOXIC dose-related adverse effects is needed.
REACTIONS PATIENT/FAMILY TEACHING
May increase risk of sphincter of Oddi
• Therapy may cause inflammation of
spasm (esp. in pts without a gallblad-
the pancreas (pancreatitis) or elevated
der), resulting in pancreatitis or hepatic
liver-associated abdominal pain, esp.
enzyme elevation that may be associated
during the first few weeks of treatment.
with or without acute abdominal pain,
Report any new or worsening abdominal
or nausea/vomiting; 80% of pts reported
pain that radiates to the back or shoul-
sphincter of Oddi spasm within the first
der, with or without nausea/vomiting.
week of treatment. May also increase risk
• Avoid chronic or acute excessive use of
of pancreatitis that is not associated with
alcohol; may increase risk of liver or pan-
sphincter of Oddi spasm. Infectious pro-
creas injury. • If a dose is missed, take
cesses including upper respiratory tract
the next dose at the regular time; do not
infection, bronchitis, nasopharyngitis,
take 2 doses at once. • Report constipa-
viral gastroenteritis were reported. May
tion lasting longer than 4 days. • Avoid
cause hypersensitivity reaction including
medications that cause constipation (e.g.,
asthma, bronchospasm, respiratory fail-
antidiarrheals, narcotics). • Report signs
ure, wheezing. Recreational abuse may
of allergic reaction; respiratory problems
produce feelings of euphoria, which may
such as worsening of asthma, bronchitis,
lead to physical dependence.
wheezing. • Drink plenty of fluids.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain baseline LFT in pts with baseline elvitegravir/­
hepatic impairment. Receive full medica- cobicistat/­
tion history and screen for interactions
requiring lower dosage. Question pt’s emtricitabine/­
usual stool characteristics (color, fre-
quency, consistency). Question history tenofovir
of alcoholism, biliary duct obstruction,
cholecystectomy, mechanical GI obstruc- el-vye-teg-ra-veer/koe-bik-i-stat/
tion, hepatic impairment, hypersensitivity em-trye-sye-ta-been/ten-oh-foe-veer
reaction, pancreatic disease, respiratory (Stribild, Genvoya)
disease, sphincter of Oddi disease or j BLACK BOX ALERT j Serious,
sometimes fatal, lactic acidosis
spasm. Assess hydration status. and severe hepatomegaly with
INTERVENTION/EVALUATION steatosis (fatty liver) have been
reported. Severe exacerbations of
Monitor for abdominal pain that radiates hepatitis B virus (HBV) reported
to the back or shoulder, with or without in pts co-infected with HIV-1 and
nausea or vomiting (esp. during first few HBV following discontinuation. If
weeks of treatment). Obtain LFT, serum discontinuation of therapy occurs,
monitor hepatic function for at

Canadian trade name Non-Crushable Drug High Alert drug


406 elvitegravir/­cobicistat/­emtricitabine/­tenofovir
least several mos. Initiate anti-HBV ric pts weighing at least 25 kg who have
therapy if warranted. had no antiretroviral treatment history
Do not confuse elvitegravir/cobi- or to replace the current antiretroviral
cistat/emtricitabine/tenofovir DF regimen in those who are virologically
(Stribild) with elvitegravir/co- suppressed (HIV-1 RNA less than 50
bicistat/emtricitabine/tenofovir copies/mL) on a stable antiretroviral
TAF (Genvoya), emtricitabine/ regimen for at least 6 mos with no his-
E rilpivirine/tenofovir (Complera), tory of treatment failure and no known
efavirenz/emtricitabine/tenofo- substitutions associated with resistance
vir (Atripla), or emtricitabine/ to the individual drug components.
tenofovir (Truvada).
PRECAUTIONS
FIXED-COMBINATION(S) Contraindications: Hypersensitivity to
Stribild: elvitegravir (an integrase elvitegravir, cobicistat, emtricitabine,
inhibitor)/cobicistat (an antiretroviral tenofovir. Concomitant use of alfuzosin,
booster, CYP3A inhibitor)/emtric- cisapride, ergot derivatives (e.g., ergota-
itabine/tenofovir fumarate (DF) (an mine), lovastatin, nephrotoxic agents,
antiretroviral): 150 mg/150 mg/200 other antiretrovirals, pimozide, rifampin,
mg/300 mg. Genvoya: elvitegravir salmeterol, sildenafil (when used for
(an integrase inhibitor)/cobicistat pulmonary hypertension), simvastatin,
(an antiretroviral booster, CYP3A in- St. John’s wort; sedative/hypnotics (e.g.,
hibitor)/emtricitabine/tenofovir (TAF) alprazolam, midazolam, triazolam, zol-
(nucleoside analog reverse transcrip- pidem) (may produce extreme sedation
tase inhibitors): 150 mg/150 mg/200 and/or respiratory depression). Cau-
mg/10 mg. tions: Renal/hepatic impairment, history
of pathological fracture, osteoporosis,
uCLASSIFICATION
osteopenia. Not recommended in pts
PHARMACOTHERAPEUTIC: Integrase with CrCl less than 70 mL/min (Stribild),
strand transfer inhibitor, antiretro- severe hepatic impairment, suspected
viral booster, nucleoside reverse lactic acidosis; pts with CrCl less than
transcriptase inhibitor, nucleotide 30mL/min (Genvoya).
reverse transcriptase inhibitor. CLINI-
CAL: Antiretroviral agent (anti-HIV). ACTION
Elvitegravir inhibits catalytic activity of
HIV-1 integrase (prevents integration of
USES
pro-viral gene into human DNA). Cobici-
Stribild: Complete regimen for treat- stat inhibits enzymes of CYP3A, boosting
ment of HIV-1 infection in adults and exposure of elvitegravir. Emtricitabine
pediatric pts 12 yrs and older weighing and tenofovir interfere with HIV viral
at least 35 kg who have no antiretro- RNA-dependent DNA polymerase activi-
viral treatment history or to replace ties. Therapeutic Effect: Interferes
the current antiretroviral regimen in with HIV replication.
those who are virologically suppressed
(HIV-1 RNA less than 50 copies/mL) PHARMACOKINETICS
on a stable antiretroviral regimen for Widely distributed. Elvitegravir, cobici-
at least 6 mos with no history of treat- stat metabolized in liver. Emtricitabine
ment failure and no known substitu- phosphorylated by cellular enzymes.
tions associated with resistance to the Tenofovir metabolized by enzymatic
individual drug components. Gen- hydrolysis, mediated by macrophages
voya: Complete regimen for treatment and hepatocytes. Protein binding: (elvite-
of HIV-1 infection in adults and pediat- gravir): greater than 99%; (cobicistat):

underlined – top prescribed drug


elvitegravir/­cobicistat/­emtricitabine/­tenofovir 407
98%; (emtricitabine): less than 4%; AVAILABILITY (Rx)
(tenofovir): less than 1%. Elvitegravir Fixed-Dose Combination Tablets: (Stribild):
excreted in feces (95%), urine (7%). elvitegravir/cobicistat/emtricitabine/teno­
Cobicistat excreted in feces (86%), urine fovir (DF): 150 mg/150 mg/200 mg/300 mg.
(8%). Emtricitabine excreted in urine (Genvoya): elvitegravir/cobicistat/emtri­
(70%), feces (14%). Tenofovir excreted citabine/tenofovir (TAF): 150 mg/150 mg/
primarily in urine (70–80%). Half- 200 mg/10 mg.
life: (emtricitabine): 13 hrs; (cobi- E
cistat): 4 hrs; (emtricitabine): 10 hrs; ADMINISTRATION/HANDLING
(tenofovir): 12–18 hrs. PO
• Give with food. • Administer at least
LIFESPAN CONSIDERATIONS
2 hrs before medications containing alu-
Pregnancy/Lactation: Breastfeed- minum, magnesium (supplements, ant-
ing not recommended due to risk of acids, laxatives).
postnatal HIV transmission. Emtric-
itabine, tenofovir are secreted in INDICATIONS/ROUTES/DOSAGE
breast milk. Unknown if elvitegravir, HIV Infection
cobicistat are secreted in breast milk. PO: ADULTS: (Stribild): 1 tablet once
Children: Safety and efficacy not daily. CHILDREN 12 YRS OR OLDER WEIGH-
established in children younger than ING AT LEAST 35 KG: 1 tablet once daily.
12 yrs or weighing less than 35 kg (Genvoya): PO: ADULTS: 1 tablet once
(Stribild), children weighing less than daily. CHILDREN 12 YRS OR OLDER WEIGH-
25 kg (Genvoya). Elderly: May have ING AT LEAST 25 KG: 1 tablet once daily.
increased risk of adverse reactions/
toxic reactions, osteopenia. Dosage in Renal Impairment
(Stribild): CrCl less than 70 mL/min
INTERACTIONS before initiation: Not recommended.
DRUG: May increase concentration/ CrCl less than 50 mL/min during
effect of axitinib, bortezomib, bosu- treatment: Recommend discontinua-
tinib, budesonide, cobimetinib, tion. (Genvoya): Not recommended in
dabrafenib, eletriptan, everolimus, pts with CrCl less than 30 mL/min.
ibrutinib, irinotecan, lovastatin,
lurasidone, neratinib, palbociclib, Dosage in Hepatic Impairment
pazopanib, ranolazine, regorafenib, Mild to moderate impairment: No
rivaroxaban, simvastatin, topote- dose adjustment. Severe impairment:
can, vemurafenib, vorapaxar. Car- Not recommended.
BAMazepine, OXcarbazepine may SIDE EFFECTS
decrease concentration/effect of elvite-
gravir. HERBAL: St. John’s wort may Frequent (16%–12%): Nausea, asthenia,
decrease concentration/effect of elvite- cough, diarrhea. Occasional (10%–4%):
gravir. Red yeast may increase risk of Headache, vomiting, abnormal dreams,
myopathy, rhabdomyolysis. FOOD: None abdominal pain, depression, paresthesia,
known. LAB VALUES: May increase fatigue, dyspepsia, arthralgia, neuropathy,
serum ALT, AST, amylase, bilirubin, BUN, hyperpigmentation. Rare (3%–1%): Dizzi-
cholesterol, creatine kinase (CK), creati- ness, eczema, insomnia, flatulence, som-
nine, glucose, phosphorus, triglycerides; nolence, pruritus, urticaria.
urine protein. May decrease CrCl, neu- ADVERSE EFFECTS/TOXIC
trophils. REACTIONS
May cause new or worsening renal fail-
ure including Fanconi syndrome (renal

Canadian trade name Non-Crushable Drug High Alert drug


408 elvitegravir/­cobicistat/­emtricitabine/­tenofovir
tubular injury, nonabsorption of essen- suspected. If other concomitant medica-
tial electrolytes, acids, buffers in renal tions were not discontinued or adjusted,
tubules). Renal tubular injury may lead closely monitor for adverse effects/
to rhabdomyolysis, osteomalacia, muscle toxic reactions. Assess for hepatic injury
weakness, myopathy. May decrease bone (bruising, hematuria, jaundice, right up-
mineral density, leading to pathological per abdominal pain, nausea, vomiting,
fractures. May cause redistribution/accu- weight loss). If discontinuation of drug
E mulation of body fat (lipodystrophy). regimen occurs, monitor hepatic func-
Fatal lactic acidosis, severe hepatomegaly tion for at least several months. Initiate
with steatosis (fatty liver) were reported. anti-HBV therapy if warranted. Monitor
If therapy is discontinued, pts co- for immune recovery syndrome, esp. af-
infected with hepatitis B or C virus have ter initiating treatment. Cough, dyspnea,
an increased risk for viral replication, fever, excess band cells on CBC may
worsening of hepatic function, and may indicate acute infection (WBC may be
experience hepatic decompensation and/ unreliable in pts with uncontrolled HIV
or failure. May induce immune recovery infection). Monitor daily pattern of bowel
syndrome (inflammatory response to activity, stool consistency; I&Os.
dormant opportunistic infections, such
PATIENT/FAMILY TEACHING
as Mycobacterium avium, cytomegalovi-
rus, PCP, tuberculosis, or acceleration of • Treatment does not cure HIV infec-
autoimmune disorders, including Graves’ tion nor reduce risk of transmission.
disease, polymyositis, Guillain-Barré). Practice safe sex with barrier methods
Allergic reactions including angioedema or abstinence. • Take with food (opti-
were reported. mizes absorption). • Drug resistance
can form if treatment is interrupted; do
NURSING CONSIDERATIONS not run out of supply. • As immune
system strengthens, it may respond to
BASELINE ASSESSMENT
dormant infections hidden within the
Obtain BUN, serum creatinine, CrCl, body. Report any new fever, chills, body
eGFR, CD4+ count, viral load, HIV-1 aches, cough, night sweats, shortness of
RNA level; urine glucose, urine pro- breath. • Report any signs of de-
tein. Obtain serum phosphate level in creased urine output, abdominal pain,
pts with renal impairment. Test all pts yellowing of skin or eyes, darkened
for HBV infection. Receive full medica- urine, clay-colored stools, weight
tion history (including herbal prod- loss. • Lactating females should not
ucts) and screen for contraindications/ breastfeed. • Decreased bone density
interactions. Concomitant use of other may lead to pathological fractures; re-
medications may need to be adjusted. port bone/extremity pain, suspected
Question possibility of pregnancy. Ques- fractures. • Antiretrovirals may cause
tion history of diabetes, hyperlipidemia, excess body fat in upper back, neck,
decreased mineral bone density. Offer breast, trunk, while also causing de-
emotional support. creased body fat in legs, arms,
INTERVENTION/EVALUATION face. • Take dose at least 2 hrs before
or at least 6 hrs after other medications
Monitor CD4+ count, viral load, HIV-1 containing aluminum, magnesium (sup-
RNA level for treatment effectiveness. plements, antacids, laxatives). • Do
Monitor renal function as clinically in- not take newly prescribed medications,
dicated. An increase in serum creatinine including OTC drugs, unless approved
greater than 0.4 mg/dL from baseline by doctor who originally started treat-
may indicate renal impairment. Obtain ment.
serum lactate level if lactic acidosis

underlined – top prescribed drug


empagliflozin 409

ACTION
empagliflozin Increases excretion of urinary glucose by
inhibiting reabsorption of filtered glucose
em-pa-gli-floe-zin
in kidney. Inhibits SGLT2 in proximal
(Jardiance)
renal tubule. Therapeutic Effect: Low-
Do not confuse empagliflozin
ers serum glucose levels.
with canagliflozin or dapagli-
flozin. PHARMACOKINETICS E
FIXED-COMBINATION(S) Readily absorbed following PO admin-
istration. Metabolized in liver by gluc-
Glyxambi: empagliflozin/linagliptin
uronidation. Peak plasma concentration:
(an antidiabetic): 10 mg/5 mg, 25
1.5 hrs. Protein binding: 86%. Excreted
mg/5 mg. Synjardy: Empagliflozin/
in urine (54%) and feces (41%). Half-
metFORMIN (an antidiabetic): 5
life: 12.4 hrs.
mg/500 mg, 5 mg/1000 mg, 12.5
mg/500 mg, 12.5 mg/1000 mg. LIFESPAN CONSIDERATIONS
uCLASSIFICATION Pregnancy/Lactation: Avoid use
during second or third trimester.
PHARMACOTHERAPEUTIC: Sodium-
Unknown if distributed in breast
glucose co-transporter 2 (SGLT2)
milk. Breastfeeding not recommended
inhibitor. CLINICAL: Antidiabetic.
during treatment. Children: Safety and
efficacy not established. Elderly: May
USES have increased risk for adverse reac-
Adjunctive treatment to diet and exer- tions (e.g., hypotension, syncope, dehy-
cise to improve glycemic controls dration).
in pts with type 2 diabetes mellitus. INTERACTIONS
Reduce risk of cardiovascular death in
pts with type 2 diabetes and cardiovas- DRUG: Insulin, insulin secreta-
cular disease. gogues (e.g., glyBURIDE) may
increase risk of hypoglycemia. HERBAL:
PRECAUTIONS None significant. FOOD: None known.
LAB VALUES: May increase low-density
Contraindications: History of hypersen-
sitivity to empagliflozin, other SGLT2 lipoprotein cholesterol (LDL-C), serum
inhibitors, severe renal impairment creatinine. May decrease eGFR.
(eGFR less than 30 mL/min), end-stage AVAILABILITY (Rx)
renal disease, dialysis. Cautions: Not
recommended in type 1 diabetes, dia- Tablets: 10 mg, 25 mg.
betic ketoacidosis. Concurrent use of
diuretics, other hypoglycemic medica- ADMINISTRATION/HANDLING
tions, mild to moderate renal impairment PO
(eGFR 30–59 mL/min), hypovolemia • Give without regard to food in the
(dehydration/anemia), elderly, pts with morning.
low systolic B/P, hyperlipidemia. Pts at
risk for lower leg amputation (diabetic INDICATIONS/ROUTES/DOSAGE
foot ulcers, peripheral vascular disease, Type 2 Diabetes Mellitus, Reduce Risk of
neuropathy). History of genital mycotic Cardiovascular Death
infection. Not recommended in pts with PO: ADULTS, ELDERLY: Initially, 10 mg
diabetic ketoacidosis, type 1 diabetes once daily in the morning. May increase
mellitus. to 25 mg once daily.

Canadian trade name Non-Crushable Drug High Alert drug


410 empagliflozin
Dosage in Renal Impairment periodically. Monitor for symptoms of
GFR 45 mL/min or greater: No dose ketoacidosis (e.g., dehydration, con-
adjustment. GFR less than 45 mL/min: fusion, extreme thirst, fruity breath,
Discontinue. Do not initiate. Kussmaul respirations, nausea). Pts
presenting with metabolic acidosis
Dosage in Hepatic Impairment should be screened for ketoacidosis,
Mild to severe impairment: No dose regardless of serum glucose levels. As-
E adjustment. sess for hypoglycemia (anxiety, confu-
SIDE EFFECTS sion, diaphoresis, diplopia, dizziness,
headache, hunger, perioral numbness,
Rare (4%–1.1%): Increased urination, dys- tachycardia, tremors); hyperglycemia
lipidemia, arthralgia, nausea. (fatigue, Kussmaul respirations, poly-
ADVERSE EFFECTS/TOXIC phagia, polyuria, polydipsia, nausea,
REACTIONS vomiting). Concomitant use of beta
blockers (e.g., carvedilol, metoprolol)
Symptomatic hypotension (orthostatic may mask symptoms of hypoglycemia.
hypotension, postural dizziness, syn- Monitor for acute kidney injury (dark-
cope) may occur, esp. in pts who are colored urine, flank pain, decreased
elderly, use diuretics, or have low sys- urine output, muscle aches). Screen
tolic B/P. Fatal cases of ketoacidosis have for glucose-altering conditions: fever,
occurred. Intravascular volume deple- increased activity or stress, surgical
tion/contraction may cause acute kidney procedures. Obtain dietary consult for
injury requiring dialysis. Hypoglycemic nutritional education. Encourage fluid
events were reported, esp. in pts using intake. Monitor weight, I&Os.
concomitant hypoglycemic medications
that cause hypoglycemia. Infections, PATIENT/FAMILY TEACHING
including urosepsis, pyelonephritis, UTI, • Diabetes mellitus requires lifelong
genital mycotic infections (male and control. Diet and exercise are principal
female), upper respiratory tract infec- parts of treatment; do not skip or delay
tion, may occur. May increase risk of meals. • Test blood sugar regu-
lower limb amputations. larly. • Monitor daily calorie in-
take. • When taking combination
NURSING CONSIDERATIONS drug therapy or when glucose demands
BASELINE ASSESSMENT are altered (fever, infection, trauma,
Obtain BUN, serum creatinine, eGFR, stress), have low blood sugar treatment
CrCl; capillary blood glucose, Hgb A1c; available (glucagon, oral dex-
B/P. Correct volume depletion before trose). • Do not breastfeed. • Slowly
initiation. Assess pt’s understanding of go from lying to standing to prevent
diabetes management, routine home dizziness. • Therapy may increase
glucose monitoring. Receive full medica- risk for dehydration/low blood pres-
tion history and screen for interactions. sure, which may cause kidney failure.
Question plans for breastfeeding. Ques- Immediately report decreased urina-
tion history of renal impairment. Screen tion, amber-colored urine, flank pain,
for risks of lower limb amputation (e.g., fatigue, swelling of the hands or
peripheral vascular disease, diabetic foot feet. • Genital itching may indicate
ulcers, neuropathy). yeast infection. • Report any signs of
UTI, kidney infection (e.g., burning
INTERVENTION/EVALUATION while urinating, cloudy urine, pelvic
Obtain BUN, serum creatinine, eGFR, pain, back pain).
CrCl; capillary blood glucose, Hgb A1c

underlined – top prescribed drug


emtricitabine/tenofovir 411

USES
emtricitabine/ Treatment of HIV-1 infection in adults and
tenofovir pediatric pts weighing at least 17 kg, in
combination with other antiretrovirals.
em-trye-sye-ta-been/ten-oh-foe-veer To reduce risk of sexually acquired HIV-1
(Truvada) in at-risk adults and adolescents weigh-
j BLACK BOX ALERT j Serious, ing at least 35 kg, in combination with
sometimes fatal, lactic acidosis safer sex practices for pre-exposure pro- E
and severe hepatomegaly with phylaxis (PrEP).
steatosis (fatty liver) have been
reported. Severe exacerbations of PRECAUTIONS
hepatitis B virus (HBV) reported
in pts co-infected with HIV-1 and Contraindications: ­Hypersensitivity to
HBV following discontinuation. If emtricitabine, tenofovir. Use of HIV-1
discontinuation of therapy occurs, PrEP in pts who are HIV-1 positive or
monitor hepatic function for at unknown infection status. Cautions:
least several mos. Initiate anti- Renal/hepatic impairment, history of
HBV therapy if warranted. HIV-1
PrEP must only be prescribed pathological fracture, osteoporosis,
to pts who are confirmed HIV-1 osteopenia; depression, diabetes. Not
negative prior to initiation and recommended in pts with CrCl less
who are screened periodically than 30 mL/min, ESRD requiring dialy-
during use. Drug-resistant HIV-1 sis (HIV-1 infection); pts with CrCl less
variants have occurred in pts with
undetected acute HIV-1 infection. than 60 mL/min (HIV-1 PrEP); sus-
Do not initiate HIV PrEP if symp- pected lactic acidosis.
toms of acute HIV-1 infection are
present unless negative status is ACTION
confirmed. Emtricitabine and tenofovir interfere
Do not confuse emtricitabine/ with HIV viral RNA-dependent DNA poly-
tenofovir DF (Truvada) with merase. Therapeutic Effect: Interferes
bictegravir/emtricitabine/ with HIV replication.
tenofovir (Biktarvy), elvitegra-
vir/cobicistat/emtricitabine/ PHARMACOKINETICS
tenofovir (Genvoya, Stribild), Widely distributed. Emtricitabine
emtricitabine/rilpivirine/teno- phosphorylated by cellular enzymes.
fovir (Complera), efavirenz/ Tenofovir metabolized by enzymatic
emtricitabine/tenofovir hydrolysis, mediated by macrophages
(Atripla) or emtricitabine/ and hepatocytes. Protein binding:
lopinavir/ritonavir/tenofovir (emtricitabine): less than 4%; (teno-
(Kaletra). fovir): less than 1%. Peak plasma con-
FIXED-COMBINATION(S) centration: (emtricitabine): 1–2 hrs;
(tenofovir): 1 hr. Emtricitabine excreted
Truvada: emtricitabine/tenofovir in urine (86%), feces (13%). Tenofovir
(antiretrovirals). excreted primarily in urine (70–80%).
uCLASSIFICATION Half-life: (emtricitabine): 10 hrs;
(tenofovir): 17 hrs.
PHARMACOTHERAPEUTIC: Nucleo-
side reverse transcriptase inhibitor, LIFESPAN CONSIDERATIONS
nucleoside reverse transcriptase Pregnancy/Lactation: Breastfeeding
inhibitor. CLINICAL: Antiretroviral not recommended due to risk of post-
agent (anti-HIV). natal HIV transmission. Emtricitabine,
tenofovir are secreted in breast milk.
Children: (HIV-1 infection): Safety and

Canadian trade name Non-Crushable Drug High Alert drug


412 emtricitabine/tenofovir
efficacy not established in pts weighing impairment: CrCl 30–49 mL/min:
less than 17 kg. (HIV-1 PrEP): Adoles- Decrease frequency to q48h. Severe
cents may exhibit poor compliance with impairment: CrCl less than 30 mL/
treatment; may benefit with more fre- min: Not recommended.
quent visits/counseling. Elderly: Not
specified; use caution. Dosage in Hepatic Impairment
Mild to severe impairment: Not
E INTERACTIONS specified; use caution.
DRUG: NSAIDs (e.g., ibuprofen, SIDE EFFECTS
ketorolac, naproxen) may enhance
nephrotoxic effects of tenofovir. Strong Occasional (9%–5%): Fatigue, nausea,
CYP3A4 inducers (e.g., carBAM- diarrhea, dizziness, rash (exfoliative,
azepine, phenytoin, rifAMPin) generalized, macular, maculo-papular,
may decrease concentration/effect. vesicular), pruritus, headache, insomnia.
HERBAL: St. John’s wort may decrease Rare (2%): Vomiting.
concentration/effect. FOOD: None ADVERSE EFFECTS/TOXIC
known. LAB VALUES: May increase REACTIONS
serum alkaline phosphatase, ALT/AST,
amylase, cholesterol, creatine kinase If therapy is discontinued, pts co-
(CK), creatinine, glucose, phospho- infected with hepatitis B or C virus have
rus, triglycerides; urine glucose. May an increased risk for viral replication,
decrease Hgb, neutrophils; CrCl. worsening of hepatic function, and may
experience hepatic decompensation and/
AVAILABILITY (Rx) or failure. May cause new or worsening
Fixed-Dose Combination Tablets: (emtric- renal failure including Fanconi syndrome
itabine/tenofovir): 100 mg/150 mg, (renal tubular injury, nonabsorption
133 mg/200 mg, 167 mg/250 mg, 200 of essential electrolytes, acids, buffers
mg/300 mg. in renal tubules). Renal tubular injury
may lead to rhabdomyolysis, osteoma-
ADMINISTRATION/HANDLING lacia, muscle weakness, myopathy. May
PO decrease bone mineral density, leading
• Give without regard to food. to pathological fractures. May cause
redistribution/accumulation of body fat
INDICATIONS/ROUTES/DOSAGE (lipodystrophy). Fatal lactic acidosis,
HIV-1 Prophylaxis (PrEP) severe hepatomegaly with steatosis (fatty
PO: ADULTS, ADOLESCENTS WEIGHING AT liver) were reported. May induce immune
LEAST 35 KG: 1 tablet (200 mg/300 mg) recovery syndrome (inflammatory
once daily. response to dormant opportunistic infec-
tions, such as Mycobacterium avium,
HIV-1 Infection (established) cytomegalovirus, PCP, tuberculosis, or
PO: ADULTS, CHILDREN WEIGHING AT acceleration of autoimmune disorders,
LEAST 35 KG: 1 tablet (200 mg/300 mg) including Graves’ disease, polymyositis,
once daily. WEIGHING 28–34 KG: 1 tablet Guillain-Barré). Use of HIV-1 PrEP in
(167 mg/250 mg) once daily. WEIGH- pts who are HIV-1 positive may develop
ING 22–27 KG: 1 tablet (133 mg/200 mg) HIV-1 resistance ­ substitutions because
once daily. WEIGHING 17–21 KG: 1 tablet prophylactic therapy is not a complete
(100 mg/150 mg) once daily. treatment regimen. Depression occurred
in 9% of pts. Upper respiratory tract
Dosage in Renal Impairment infection, sinusitis were reported in 8%
Mild impairment: CrCl 50–80 mL/ of pts.
min: No dose adjustment. Moderate

underlined – top prescribed drug


emtricitabine/tenofovir 413

NURSING CONSIDERATIONS several months. Initiate anti-HBV ther-


apy if warranted. Monitor for immune
BASELINE ASSESSMENT recovery syndrome, esp. after initiat-
Obtain BUN, serum creatinine, CrCl, ing treatment. Cough, dyspnea, fever,
eGFR; urine glucose, urine protein. Ob- excess band cells on CBC may indicate
tain CD4+ count, viral load, HIV-1 RNA acute infection (WBC may be unreliable
level (if therapy used to treat known in pts with uncontrolled HIV infection).
HIV-1 infection). Obtain serum phos- Monitor daily pattern of bowel activity, E
phate level in pts with renal impair- stool consistency; I&Os. Monitor for
ment. Test all pts for HBV infection. For symptoms of depression (fatigue, flat
HIV-1 PrEP, a negative HIV-1 test must affect, irritability, feelings of sadness,
be confirmed before initiation. If recent hopelessness, suicidal ideation). For
exposure is suspected (less than 1 mo) HIV-1 PrEP, test for HIV-1 infection at
or if symptoms of acute HIV-1 infection least q3mos. If symptoms of acute HIV-1
are present (e.g., fatigue, fever, lymph- infection are present or screening indi-
adenopathy, myalgia, rash), delay initia- cates possible infection, consider con-
tion for at least 1 mo until HIV-1 status version to full treatment regimen until
is confirmed. When considering HIV-1 an approved test has confirmed nega-
PrEP, screen for high-risk factors includ- tive status.
ing HIV-1 infected partners, sexual activ- PATIENT/FAMILY TEACHING
ity with high-prevalence area or social
network and additional risk factors (e.g., • Treatment does not cure HIV infection
drug or alcohol dependence, incarcera- or reduce risk of transmission. Practice
tion, noncompliant condom use, previ- safe sex with barrier methods or absti-
ous STD infections; sexual exchanges for nence. • Drug resistance can form if
food, money, shelter, drugs; sexual part- treatment is interrupted; do not run out
ners with unknown HIV-1 status who are of supply. • Report any signs of de-
at risk of infection). Question potential creased urine output, abdominal pain,
exposures (unprotected sexual activity, yellowing of skin or eyes, darkened
sexual activity with HIV-1 infected part- urine, clay-colored stools, weight
ner, breakage of condom). Question loss. • Lactating females should not
possibility of pregnancy. Question history breastfeed. • Decreased bone density
of diabetes, depression, hyperlipidemia, may lead to pathological fractures; re-
decreased mineral bone density. Offer port bone/extremity pain, suspected
emotional support. fractures. • Antiretrovirals may cause
excess body fat in upper back, neck,
INTERVENTION/EVALUATION breast, trunk, while also causing de-
Monitor CD4+ count, viral load, HIV-1 creased body fat in legs, arms,
RNA level for treatment effectiveness face. • Do not take newly prescribed
(if therapy used to treat known HIV-1 medications, including OTC drugs, un-
infection). Monitor renal function as less approved by doctor who originally
clinically indicated. An increase in se- started treatment.
rum creatinine greater than 0.4 mg/ • HIV-1 Prep: Despite preventative
dL from baseline may indicate renal treatment, safer sex practices with con-
impairment. Obtain serum lactate level doms and risk reduction must be
if lactic acidosis suspected. Assess for used. • A negative HIV test result must
hepatic injury (bruising, hematuria, be obtained before initiation. • HIV
jaundice, right upper abdominal pain, ­status tests will be performed q3mos (or
nausea, vomiting, weight loss). If dis- more frequently) after starting treat-
continuation of drug regimen occurs, ment. • If possible transmission or
monitor hepatic function for at least symptoms of HIV infection occur, therapy

Canadian trade name Non-Crushable Drug High Alert drug


414 enalapril
must be interrupted, and a complete HIV hypertension in adults and children
treatment regimen may be started until a older than 1 mo. OFF-LABEL: Protein-
negative HIV status test is con- uria in steroid-resistant nephrotic
firmed. • Report symptoms of HIV in- syndrome.
fection such as diarrhea, fatigue, fever,
myalgia, night sweats, rash, swelling of PRECAUTIONS
lymph nodes. • Immediately report Contraindications: Hypersensitivity to
E breakage of condom, sexual activity with enalapril. History of angioedema from
partner suspected of HIV infection, diag- previous treatment with ACE inhibi-
nosis of STD, sexual practices that in- tors. Idiopathic/hereditary angio-
crease risk for infection (inconsistent edema. Concomitant use of aliskiren
condom usage, multiple partners, alco- in pts with diabetes. Coadministration
hol/drug dependence; sex in exchange with or within 36 hrs of switching to
for money, shelter, food, drugs). • Stay or from a neprilysin inhibitor (e.g.,
compliant with preventative treatment sacubitril). Cautions: Renal impair-
regimen. Missing doses may increase ment, hypertrophic cardiomyopathy
risk of HIV transmission/infection. with outflow tract obstruction; severe
aortic stenosis; before, during, or
immediately after major surgery. Con-
comitant use of potassium supplement;
enalapril unstented unilateral or bilateral renal
artery stenosis.
en-al-a-pril
(Epaned, Vasotec) ACTION
j BLACK BOX ALERT jMay Suppresses renin-angiotensin-aldo-
cause fetal injury. Discontinue as sterone system (prevents conversion
soon as possible once pregnancy
is detected. of angiotensin I to angiotensin II, a
Do not confuse enalapril with potent vasoconstrictor; may inhibit
Anafranil, Elavil, Eldepryl, angiotensin II at local vascular, renal
lisinopril, or ramipril. sites). Decreases plasma angioten-
sin II, increases plasma renin activ-
FIXED-COMBINATION(S) ity, decreases aldosterone secretion.
Lexxel: enalapril/felodipine (cal- Therapeutic Effect: In hyperten-
cium channel blocker): 5 mg/2.5 sion, reduces peripheral arterial resis-
mg, 5 mg/5 mg. Teczem: enalapril/ tance. In HF, increases cardiac output;
dilTIAZem (calcium channel blocker): decreases peripheral vascular resis-
5 mg/180 mg. Vaseretic: enalapril/ tance, B/P, pulmonary capillary wedge
hydroCHLOROthiazide (diuretic): 5 pressure, heart size.
mg/12.5 mg, 10 mg/25 mg.
PHARMACOKINETICS
uCLASSIFICATION Route Onset Peak Duration
PHARMACOTHERAPEUTIC: Angio- PO 1 hr 4–6 hrs 24 hrs
tensin-converting enzyme (ACE) in- IV 15 min 1–4 hrs 6 hrs
hibitor. CLINICAL: Antihypertensive.
Readily absorbed from GI tract. Pro-
drug undergoes hepatic biotrans-
USES formation to enalaprilat. Protein
Treatment of hypertension alone or binding: 50%–60%. Primarily excreted
in combination with other antihyper- in urine. Removed by hemodialysis.
tensives. Adjunctive therapy for symp- Half-life: 11 hrs (increased in renal
tomatic HF. Epaned: Treatment of impairment).
underlined – top prescribed drug
enalapril 415

LIFESPAN CONSIDERATIONS Amphotec), cefepime (Maxipime), phe-


Pregnancy/Lactation: Crosses pla- nytoin (Dilantin).
centa. Distributed in breast milk. May IV COMPATIBILITIES
cause fetal/neonatal mortality, morbidity.
Children: Safety and efficacy not estab-
Calcium gluconate, dexmedetomidine
lished. Elderly: May be more suscep- (Precedex), DOBUTamine (Dobutrex),
tible to hypotensive effects. DOPamine (Intropin), fentaNYL (Subli-
maze), heparin, lidocaine, magnesium E
INTERACTIONS sulfate, morphine, nitroglycerin, potas-
DRUG: Aliskiren may increase hyper- sium chloride, potassium phosphate,
kalemic effect. May increase potential propofol (Diprivan).
for hypersensitivity reactions to allopu- INDICATIONS/ROUTES/DOSAGE
rinol. Angiotensin receptor block-
Hypertension
ers (e.g., losartan, valsartan) may
increase adverse effects. May increase PO: ADULTS, ELDERLY: Initially, 2.5–5
adverse effects of lithium, sacubitril. mg/day (2.5 mg if pt taking a diuretic).
HERBAL: Herbals with hypertensive
May increase at 1–2 wk intervals.
properties (e.g., licorice, yohimbe) Range: 10–40 mg/day in 1–2 divided
or hypotensive properties (e.g., doses. CHILDREN 1 MO–16 YRS: Initially,
garlic, ginger, ginkgo biloba) may 0.08 mg/kg once daily. Adjust dose
alter effects. FOOD: None known. LAB based on pt response. Maximum: 5
VALUES: May increase serum BUN, alka-
mg/day. NEONATES: 0.04–0.1 mg/kg/
line phosphatase, bilirubin, creatinine, day given q24h.
IV: ADULTS, ELDERLY: 0.625–1.25 mg
potassium, ALT, AST. May decrease serum
sodium. May cause positive ANA titer. q6h up to 5 mg q6h.
Adjunctive Therapy for HF
AVAILABILITY (Rx)
PO: ADULTS, ELDERLY: Initially, 2.5
Injection Solution: 1.25 mg/mL. Powder mg twice daily. Titrate slowly at 1–2
for Oral Solution: (Epaned): 1 mg/mL. Tab- wk intervals. Range: 5–40 mg/day in 2
lets: 2.5 mg, 5 mg, 10 mg, 20 mg. divided doses. Target: 10–20 mg twice
ADMINISTRATION/HANDLING daily.

IV Dosage in Renal Impairment


CrCl greater than 30 mL/min: No
Reconstitution • May give undiluted dosage adjustment. CrCl 30 mL/min
or dilute with D5W or 0.9% NaCl. or less: (HTN): Initially, 2.5 mg/day.
Rate of administration • For IV Titrate until B/P controlled. (HF): Initially,
push, give undiluted over 5 min. • For 2.5 mg twice daily. May increase by 2.5
IV piggyback, infuse over 10–15 min. mg/dose at greater than 4-day i­ntervals.
Storage • Store parenteral form at Maximum: 40 mg/day. Hemodialy-
room temperature. • Use only clear, sis: Initially, 2.5 mg on dialysis days;
colorless solution. • Diluted IV solution adjust dose on non-dialysis days depend-
is stable for 24 hrs at room temperature. ing on B/P.
PO Dosage in Hepatic Impairment
• Give without regard to food. • Tab- No dose adjustment.
lets may be crushed.
SIDE EFFECTS
IV INCOMPATIBILITIES Frequent (7%–5%): Headache, dizzi-
Amphotericin B (Fungizone), ampho- ness. Occasional (3%–2%): Orthostatic
tericin B complex (Abelcet, AmBisome, hypotension, fatigue, diarrhea, cough,
Canadian trade name Non-Crushable Drug High Alert drug
416 enasidenib
syncope. Rare (less than 2%): Angina,
abdominal pain, vomiting, nausea, rash, enasidenib
asthenia.
en-a-sid-a-nib
ADVERSE EFFECTS/TOXIC (Idhifa)
REACTIONS j BLACK BOX ALERT j May
Excessive hypotension (“first-dose syn- cause differentiation syndrome (a
E condition of life-threatening compli-
cope”) may occur in pts with HF, severe cations caused by chemotherapy),
salt or volume depletion. Angioedema which can be fatal if not treated.
(facial, lip swelling), hyperkalemia If differentiation syndrome is
occur rarely. Agranulocytosis, neutro- suspected, consider treatment with
penia may be noted in pts with renal a corticosteroid and hemodynamic
monitoring.
impairment, collagen vascular diseases
(scleroderma, systemic lupus erythe- Do not confuse enasidenib
matosus). Nephrotic syndrome may with cobimetinib, dabrafenib,
be noted in those with history of renal encorafenib, ivosidenib,
disease. ­regorafenib, or trametinib.
uCLASSIFICATION
NURSING CONSIDERATIONS
PHARMACOTHERAPEUTIC: Isoci-
BASELINE ASSESSMENT trate dehydrogenase-2 (IDH2) in-
Obtain BUN, serum creatinine, CrCL. hibitor. CLINICAL: Antineoplastic.
Receive full medication history, esp.
potassium-sparing diuretics. Obtain
B/P immediately before each dose (be USES
alert to fluctuations). In pts with re- Treatment of adults with relapsed or
nal impairment, autoimmune disease, refractory acute myeloid leukemia (AML)
or taking drugs that affect leukocytes/ with an isocitrate dehydrogenase-2
immune response, CBC should be (IDH2) mutation.
performed before beginning therapy,
q2wks for 3 mos, then periodically PRECAUTIONS
thereafter. Contraindications: Hypersensitivity to
enasidenib. Cautions: Hepatic/renal
INTERVENTION/EVALUATION impairment, dehydration; pts at high risk
Assist with ambulation if dizziness oc- for tumor lysis syndrome (high tumor
curs. Monitor CBC, serum BUN, potas- burden).
sium, creatinine, B/P. Monitor daily pat-
tern of bowel activity, stool consistency. ACTION
PATIENT/FAMILY TEACHING
Inhibits isocitrate dehydrogenase-2
(IDH2) enzymes on mutant IDH2
• To reduce hypotensive effect, go variants, decreasing 2-hydroxyglu-
from lying to standing slowly. • Sev- tarate (2-HG) levels and restoring
eral wks may be needed for full thera- myeloid differentiation. Therapeutic
peutic effect of B/P reduction. • Skip- Effect: Reduces blast counts; increases
ping doses or voluntarily discontinuing percentage of myeloid cells. Inhibits
drug may produce severe rebound hy- tumor growth and proliferation.
pertension. • Limit alcohol in-
take. • Report vomiting, diarrhea, PHARMACOKINETICS
diaphoresis, persistent cough, diffi- Widely distributed. Metabolized in liver.
culty in breathing; swelling of face, Protein binding: 99%. Peak plasma con-
lips, tongue. centration: 4 hrs. Steady state reached in

underlined – top prescribed drug


enasidenib 417
29 days. Excreted in feces (89%), urine hemodynamic monitoring. Pulmonary
(11%). Half-life: 137 hrs. failure requiring intubation or ven-
tilation, renal dysfunction persisting
LIFESPAN CONSIDERATIONS greater than 48 hrs (despite treat-
Pregnancy/Lactation: Avoid preg- ment with a corticosteroid): With-
nancy; may cause fetal harm. Females hold treatment until improved to Grade 2
of reproductive potential and males with or less, then resume at 100 mg once daily.
female partners of reproductive potential E
should use effective contraception dur- Hepatotoxicity
ing treatment and for at least 1 mo after Serum bilirubin elevation greater than
discontinuation. Unknown if distributed 3 times ULN for more than 2 wks (in
in breast milk. Breastfeeding not recom- the absence of transaminase eleva-
mended during treatment and for at least tion or other hepatic injury): Reduce
1 mo after discontinuation. May impair dose to 50 mg once daily. If serum bilirubin
fertility in both females and males of improves to less than 2 times ULN, increase
reproductive potential. Children: Safety dose to 100 mg once daily.
and efficacy not established. Elderly: No Noninfectious Leukocytosis
age-related precautions noted. WBC greater than 30,000 cells/
mm3: Consider therapy with hydroxy-
INTERACTIONS
urea. If leukocytosis does not improve
DRUG: None significant. HERBAL: None with hydroxyurea therapy, withhold ena-
significant. FOOD: None known. LAB sidenib until WBC improves to less than
VALUES: May increase serum bilirubin; 30,000/mm3, then resume enasidenib at
WBC. May decrease serum calcium, 100 mg once daily.
potassium, phosphorus.
Any Other Toxicity
AVAILABILITY (Rx) Any Grade 3 or 4 toxicity related
Tablets: 50 mg, 100 mg. to treatment (tumor lysis syn-
drome): Withhold treatment until resolved
ADMINISTRATION/HANDLING to Grade 2 or less, then resume at 50 mg
PO once daily. If toxicities resolve to Grade 1 or
• Give without regard to food. • Ad- 0, increase dose to 100 mg once daily.
minister whole; do not cut, crush, or di- Dosage in Renal Impairment
vide tablets. CrCl greater than 30 mL/min: No
INDICATIONS/ROUTES/DOSAGE dose adjustment. CrCl less than 30
mL/min: Not specified; use caution.
Acute Myeloid Leukemia
PO: ADULTS, ELDERLY: 100 mg once daily. Dosage in Hepatic Impairment
Continue until disease progression or Mild impairment: No dose adjustment.
unacceptable toxicity. For pts without dis- Moderate to severe impairment: Not
ease progression or unacceptable toxic- specified; use caution.
ity, treat for a minimum of 6 mos (allows
time for clinical response). SIDE EFFECTS
Frequent (50%–25%): Nausea, diarrhea,
Dose Modification
vomiting, decreased appetite, dysgeusia.
Based on Common Terminology Criteria
for Adverse Events (CTCAE). ADVERSE EFFECTS/TOXIC
Differentiation Syndrome
REACTIONS
If differentiation syndrome is suspected, Life-threatening differentiation syndrome
treat with a systemic corticosteroid and (bone pain, dyspnea, fever, lymphade-

Canadian trade name Non-Crushable Drug High Alert drug


418 encorafenib
nopathy, peripheral edema, plural/peri- joint pain, palpitations, seizures, vomit-
cardial effusion, pulmonary infiltrates, ing. • Treatment may cause differentiation
rapid weight gain, respiratory distress; syndrome (a condition of life-threatening
hepatic/renal/multi-organ dysfunction) complications caused by induction chemo-
reported in 14% of pts; may occur 10 therapy), which can be fatal. Report bone
days to 5 mos after initiation. Noninfec- pain, difficulty breathing, fever, swelling of
tious leukocytosis reported in 12% of the lymph nodes or extremities, lung con-
E pts. Tumor lysis syndrome may present gestion or infection, organ dysfunction,
as acute renal failure, hypocalcemia, rapid weight gain. • Avoid pregnancy. Use
hyperuricemia, hyperphosphatemia. effective contraception during treatment and
Acute respiratory distress syndrome, for at least 1 mo after last dose. Do not
pulmonary edema occurred in less than breastfeed during treatment and for at least
10% of pts. 1 mo after last dose. • Report treatment-
induced liver toxicity such as bruising, con-
NURSING CONSIDERATIONS fusion; amber, dark, orange-colored urine;
BASELINE ASSESSMENT right upper abdominal pain, yellowing of the
skin or eyes. • Nausea, vomiting, diarrhea
Obtain WBC; pregnancy test in females of are common side effects. Drink plenty of
reproductive potential. Verify presence fluids.
of IDH2 mutations in the blood or bone
marrow. Question plans of breastfeeding.
Confirm compliance of effective contra-
ception. Due to increased risk of tumor
lysis syndrome, diarrhea, vomiting, as-
encorafenib
sess adequate hydration before initiation. en-koe-raf-e-nib
Offer emotional support. (Braftovi)
INTERVENTION/EVALUATION Do not confuse encorafenib
Monitor WBC for leukocytosis; BMP, se- with binimetinib, cobimetinib,
rum calcium, phosphate, uric acid for dabrafenib, dasatinib, erlotinib,
tumor lysis syndrome (acute renal fail- trametinib, or vemurafenib, or
ure, electrolyte imbalance, cardiac ar- Braftovi with Mektovi.
rhythmias, seizures) q2wks for the first uCLASSIFICATION
3 mos. Monitor LFT for transaminitis,
hepatotoxicity periodically. If differen- PHARMACOTHERAPEUTIC: BRAF
tiation syndrome is suspected, consider kinase inhibitor. CLINICAL: Antineo-
treatment with a corticosteroid and he- plastic.
modynamic monitoring. Once symptoms
have resolved, taper corticosteroid ther- USES
apy. Offer antiemetic if nausea occurs;
antidiarrheal if diarrhea occurs. Moni- Treatment of pts with unresectable or
tor daily pattern of bowel activity, stool metastatic melanoma with a BRAF V600E
consistency. Ensure adequate hydration, or V600K mutation (in combination with
nutrition. Monitor weight, I&Os. binimetinib). OFF-LABEL: Treatment of
colorectal cancer, metastatic, refractory
PATIENT/FAMILY TEACHING (RAS wild-type, BRAF V600E-mutant.
• Therapy may cause tumor lysis syndrome
(a condition caused by the rapid breakdown PRECAUTIONS
of cancer cells), which can cause kidney Contraindications: Hypersensitivity to en-
failure and can be fatal. Report decreased corafenib. Cautions: Baseline anemia,
urination, amber-colored urine, confusion, leukopenia, lymphopenia, neutropenia;
difficulty breathing, fatigue, fever, muscle or active infection; conditions predisposing

underlined – top prescribed drug


encorafenib 419
to infection (e.g., diabetes, renal failure, azithromycin, haloperidol, sotalol)
immunocompromised pts, open may increase risk of QTc interval prolon-
wounds), diabetes, hepatic/renal impair- gation. HERBAL: None significant. FOOD:
ment; pts at risk for QTc interval prolon- Grapefruit products may increase
gation (congenital long QT syndrome, concentration/effect; avoid use. LAB
HF, mediations that prolong QTc interval, VALUES: May increase serum alkaline
hypokalemia, hypomagnesemia): con- phosphatase, ALT, AST, creatinine, GGT,
comitant use of strong or moderate glucose, magnesium. May decrease E
CYP3A inhibitors or strong or moderate serum sodium; Hct, Hgb, leukocytes,
CYP3A inducers. lymphocytes, neutrophils, RBCs.
ACTION AVAILABILITY (Rx)
An ATP-competitive inhibitor of protein Capsules: 75 mg.
kinase BRAF. Therapeutic Effect: Inhib-
its tumor cell growth. ADMINISTRATION/HANDLING
PO
PHARMACOKINETICS • Give without regard to food. • If a
Widely distributed. Metabolized in liver. dose is missed or vomiting occurs after
Protein binding: 86%. Peak plasma con- administration, give next dose at regu-
centration: 2 hrs. Steady state reached in larly scheduled time • Do not give a
15 days. Excreted in urine (47%), feces missed dose within 12 hrs of next
(47%). Half-life: 3.5 hrs. dose. • Administer whole; do not
break, cut, or open capsule. Capsule
LIFESPAN CONSIDERATIONS cannot be chewed.
Pregnancy/Lactation: Avoid preg-
nancy; may cause fetal harm. Female pts INDICATIONS/ROUTES/DOSAGE
of reproductive potential must use effec- Metastatic Melanoma
tive nonhormonal contraception (e.g., PO: ADULTS, ELDERLY: 450 mg once daily
barrier methods) during treatment and (in combination with binimetinib). Con-
for at least 2 wks after discontinuation. tinue until disease progression or unac-
Unknown if distributed in breast milk. ceptable toxicity. If binimetinib withheld,
Breastfeeding not recommended during reduce encorafenib dose to 300 mg until
treatment and for at least 2 wks after dis- binimetinib is restarted.
continuation. Males: May impair fertility.
Children: Safety and efficacy not estab- Dose Reduction for Adverse Reactions
lished. Elderly: No age-related precau- First dose reduction: 300 mg once
tions noted. daily. Second dose reduction: 225 mg
once daily. Unable to tolerate 225 mg
INTERACTIONS dose: Permanently discontinue.
DRUG: Strong CYP3A4 inhibitors
Dose Modification
(e.g., clarithromycin, ketocon-
azole), moderate CYP3A4 inhibi- Based on Common Terminology Criteria
tors (e.g., ciprofloxacin, dilTIAZem, for Adverse Events (CTCAE). See pre-
fluconazole, verapamil) may increase scribing information for binimetinib for
concentration/effect. Strong CYP3A4 recommended dose modification.
inducers (e.g., carBAMazepine, Dermatologic Reactions
phenytoin, rifAMPin) may decrease Grade 2 skin reaction: If not improved
concentration/effect. May decrease within 2 wks, withhold treatment until
concentration/effect of oral contra- improved to Grade 1 or 0, then resume
ceptives. QT interval–prolonging at same dose. Grade 3 skin reaction:
medications (e.g., amiodarone, Withhold treatment until improved to
Canadian trade name Non-Crushable Drug High Alert drug
420 encorafenib
Grade 1 or 0, then resume at same dose Consider permanent discontinuation.
for first occurrence or at reduced dose Recurrent Grade 4 reaction: Perma-
for subsequent occurrence. Grade 4 nently discontinue.
skin reaction: Permanently discontinue.
Concomitant Use with CYP3A Inhibitors
Hepatotoxicity If strong CYP3A inhibitor cannot be dis-
Grade 2 serum ALT, AST elevation: continued, reduce dose to one-third of
E Maintain dose. If not improved within 4 the dose prior to use of strong CYP3A
wks, withhold treatment until improved inhibitor. If moderate CYP3A inhibitor
to Grade 1 or 0 (or to pretreatment base- cannot be discontinued, reduce dose to
line), then resume at same dose. Grade one-half of the dose prior to use of mod-
3 or 4 serum ALT, AST elevation: See erate CYP3A inhibitor. If CYP3A inhibitor
Other Adverse Reactions. is discontinued for 3–5 half-lives, may
resume dose prior to starting CYP3A in-
New Primary Malignancies hibitor.
Noncutaneous RAS mutation–posi-
tive malignancies: Permanently dis- Dosage in Renal Impairment
continue. Mild impairment: No dose adjustment.
Moderate to severe impairment: Not
QTc Interval Prolongation specified; use caution.
QTcF interval greater than 500 msec
and less than or equal to 60 msec Dosage in Hepatic Impairment
from baseline: Withhold treatment until Mild to moderate impairment: No
QTcF is less than or equal to 500 msec, dose adjustment. Severe impairment:
then resume at reduced dose. QTcF Not specified; use caution.
interval greater than 500 msec and
greater than 60 msec from baseline: SIDE EFFECTS
Permanently discontinue. Frequent (43%-14%): Fatigue, nausea,
vomiting, abdominal pain, arthralgia,
Uveitis hyperkeratosis, myopathy, rash, head-
Grade 1 or 2 uveitis that does not ache, constipation, pyrexia, dry skin, diz-
respond to ocular therapy; Grade ziness, alopecia. Occasional (13%–3%):
3 uveitis: Withhold treatment for up to Pruritus, peripheral neuropathy, extrem-
6 wks. If symptoms improve, resume at ity pain, dysgeusia, acneiform dermatitis.
same or reduced dose. If not improved,
permanently discontinue. ADVERSE EFFECTS/TOXIC
REACTIONS
Other Adverse Reactions (including
Anemia, leukopenia, lymphopenia, neu-
Hemorrhage)
tropenia is an expected response to
Any recurrent Grade 2 reaction; first
therapy. In pts receiving combination
occurrence of any Grade 3 reaction:
therapy, new primary cutaneous malig-
Withhold treatment for up to 4 wks. If nancies including cutaneous squamous
improved to Grade 1 or 0 (or to pretreat- cell carcinoma (including keratoacan-
ment baseline), resume at reduced dose. thoma) (3% of pts), basal cell carci-
If not improved, permanently discon- noma (2% of pts) have occurred. In pts
tinue. First occurrence of any Grade receiving single-agent therapy, new pri-
4 reaction: Permanently discontinue
mary cutaneous malignancies including
or withhold treatment for up to 4 wks. cutaneous squamous cell carcinoma (in-
If improved to Grade 1 or 0 (or to pre- cluding keratoacanthoma) (8% of pts),
treatment baseline), resume at reduced basal cell carcinoma (1% of pts), new
dose. If not improved, permanently dis- primary melanoma (5% of pts) have
continue. Recurrent Grade 3 reaction:

underlined – top prescribed drug


encorafenib 421
occurred. May increase potential for new longation. Assess skin for new lesions,
primary noncutaneous malignancies as- toxicities q2mos during treatment and up
sociated with activation of RAS through to 6 mos after discontinuation. Assess for
mutation. May increase cellular prolifer- eye pain/redness, visual changes at each
ation of BRAF wild-type cells and activate office visit and at regular intervals. Moni-
MAP-kinase signaling. Serious hemor- tor for toxicities if discontinuation of
rhagic events including GI bleeding, rec- CYP3A inhibitor or CYP3A inducer is un-
tal bleeding (4% of pts), hematochezia avoidable. Monitor for signs of hypergly- E
(3% of pts), hemorrhoidal hemorrhage cemia (thirst, polyuria, confusion, dehy-
(1% of pts) were reported. Fatal intra- dration). If QT interval–prolonging
cranial hemorrhage reported in 2% of medications cannot be withheld, dili-
pts in the setting of new or progressive gently monitor ECG for QT interval pro-
brain metastasis. Uveitis, including iritis longation, cardiac arrhythmias. Monitor
and iridocyclitis, occurred in 4% of pts. for GI bleeding, bloody stool; symptoms
QTc interval prolongation reported in 1% of intracranial bleeding (aphasia, blind-
of pts. Grade 3 or 4 dermatologic toxici- ness, confusion, facial droop, hemiple-
ties reported in 21% of pts when used as gia, seizures). Diligently screen for infec-
a single agent. Other reactions occurring tions.
in less than 10% of pts include facial pa-
resis, pancreatitis, panniculitis, drug hy- PATIENT/FAMILY TEACHING
persensitivity. • Treatment may depress your immune
system and reduce your ability to fight
NURSING CONSIDERATIONS infection. Report symptoms of infection
such as body aches, chills, cough, fa-
BASELINE ASSESSMENT
tigue, fever. Avoid those with active infec-
Obtain CBC, BMP, LFTs; pregnancy test in tion. • Expect frequent eye exams, skin
female pts of reproductive potential. Con- exams. • Report any vision changes,
firm compliance of effective nonhor- eye redness.
monal contraception. Correct hypokale- • Treatment may cause new skin can-
mia, hypomagnesemia prior to and cers. Report new warts, moles. • Re-
during treatment. Confirm presence of port symptoms of liver problems (bruis-
BRAF V600E or V600K mutation in tumor ing, confusion; dark, amber- or
specimen. Perform full dermatologic orange-colored urine; right upper ab-
exam; assess skin for moles, lesions, dominal pain, yellowing of the skin or
papillomas. Consider baseline ECG in pts eyes); hemorrhagic stroke (confusion,
at risk for QTc interval prolongation. difficulty speaking, one-sided weakness
Receive full medication history and or paralysis, loss of vision), GI bleeding
screen for interactions (esp. QTc inter- such (bloody stools, rectal bleed-
val–prolonging medications). Question ing). • Female pts of childbearing po-
history of diabetes, hepatic/renal impair- tential should use effective nonhormonal
ment, HF. Screen for active infection. Of- contraception during treatment and for
fer emotional support. at least 2 wks after last dose. • Do not
breastfeed. • Avoid grapefruit prod-
INTERVENTION/EVALUATION
ucts, herbal supplements (esp. St. John’s
Monitor CBC for anemia, leukopenia, wort). • Report palpitations, chest
lymphopenia, neutropenia; LFT for hepa- pain, shortness of breath, dizziness, faint-
totoxicity (bruising, hematuria, jaundice, ing; may indicate arrhythmia. • Do not
right upper abdominal pain, nausea, take newly prescribed medications un-
vomiting, weight loss); serum potassium, less approved by prescriber who origi-
magnesium in pts with QTc interval pro- nally started therapy.

Canadian trade name Non-Crushable Drug High Alert drug


422 enoxaparin
neuraxial anesthesia (epidural or spinal
enoxaparin anesthesia) or spinal puncture is used,
pts anticoagulated or scheduled to be
en-ox-a-par-in anticoagulated with enoxaparin for pre-
(Lovenox) vention of thromboembolic complications
j BLACK BOX ALERT jEpidural are at risk for developing an epidural or
or spinal anesthesia greatly in- spinal hematoma that can result in long-
E creases potential for spinal or
epidural hematoma, subsequent term or permanent paralysis. Bacterial
long-term or permanent paralysis. endocarditis, hemorrhagic stroke, history
Do not confuse Lovenox with of ­ heparin-induced thrombocytopenia
Lasix, Levaquin, Lotronex, or (HIT), severe hepatic disease.
Protonix, or enoxaparin with
dalteparin or heparin. ACTION
Enhances the inhibition rate of clotting
uCLASSIFICATION proteases by antithrombin III. Impairs
PHARMACOTHERAPEUTIC: Low normal hemostasis and inhibition of fac-
molecular weight heparin. CLINI- tor Xa. Therapeutic Effect: Produces
CAL: Anticoagulant. anticoagulation. Does not significantly
influence PT, aPTT.

USES PHARMACOKINETICS
DVT prophylaxis following hip or knee Route Onset Peak Duration
replacement surgery, abdominal surgery, SQ N/A 3–5 hrs 12 hrs
or pts with severely restricted mobility dur-
ing acute illness. Treatment of acute coro- Well absorbed after SQ administration.
nary syndrome (ACS): unstable angina, Excreted primarily in urine. Not removed
non–Q-wave MI, acute ST-segment eleva- by hemodialysis. Half-life: 4.5–7 hrs.
tion MI (STEMI). Treatment of DVT with or
LIFESPAN CONSIDERATIONS
without pulmonary embolism (PE) (inpa-
tient); without PE (outpatient). OFF-LABEL: Pregnancy/Lactation: Use with cau-
DVT prophylaxis following moderate-risk tion, particularly during third trimester,
general surgery, gynecologic surgery; immediate postpartum period (increased
management of venous thromboembolism risk of maternal hemorrhage). Unknown
(VTE) during pregnancy. Bariatric surgery, if distributed in breast milk. Pregnant
mechanical heart valve to bridge anticoag- women with mechanical heart valves
ulation, percutaneous coronary interven- (and their fetuses) may have increased
tion (PCI) adjunctive therapy. risk of bleeding. Children: Safety and
efficacy not established. Elderly: May
PRECAUTIONS be more susceptible to bleeding.
Contraindications: Hypersensitivity to
INTERACTIONS
enoxaparin. Active major bleeding, con-
current heparin therapy, hypersensitiv- DRUG: Anticoagulants (e.g., apixaban,
ity to heparin, pork products. History dabigatran, edoxaban, rivaroxaban),
of heparin-induced thrombocytopenia antiplatelets (e.g., aspirin, clopido-
(HIT) in past 100 days or in the presence grel, ticagrelor), NSAIDs (ibuprofen,
of circulating antibodies. Cautions: Con- ketorolac, naproxen), thrombolytics
ditions with increased risk of hemor- (e.g., alteplase), warfarin may increase
rhage, platelet defects, renal impairment anticoagulant effect; risk of bleeding.
(renal failure), elderly, uncontrolled HERBAL: Herbals with anticoagulant/
arterial hypertension, history of recent antiplatelet activity (e.g., garlic,
GI ulceration or hemorrhage. When ginger, ginkgo biloba) may increase

underlined – top prescribed drug


enoxaparin 423
adverse effects. FOOD: None known. LAB Prevention of DVT After Non-Orthopedic
VALUES: Increases serum alkaline phos- Surgery
phatase, ALT, AST. May decrease Hgb, Hct, SQ: ADULTS, ELDERLY: 40 mg/day for
platelets, RBCs. 7–10 days, with initial dose given 2
hrs before abdominal surgery or approx-
AVAILABILITY (Rx) imately 12 hrs before other surgeries.
Injection Solution: 30 mg/0.3 mL, 40
mg/0.4 mL, 60 mg/0.6 mL, 80 mg/0.8 Prevention of DVT After Bariatric Surgery E
mL, 100 mg/mL, 120 mg/0.8 mL, 150 BMI 50 kg/m2 or less: 40 mg q12h.
mg/mL in prefilled syringes. BMI greater than 50 kg/m2: 60 mg
q12h.
ADMINISTRATION/HANDLING
Prevention of Long-Term DVT in
b ALERT c Do not mix with other injec-
Nonsurgical Acute Illness
tions, infusions. Do not give IM. SQ: ADULTS, ELDERLY: 40 mg once
SQ daily; continue until risk of DVT has
Preparation • Visually inspect for particu- diminished (usually 6–11 days).
late matter or discoloration. Solution should
Prevention of Ischemic Complications of
appear clear, colorless to pale yellow in color.
Unstable Angina, Non–Q-Wave MI (with
Do not use if solution is cloudy, discolored, or
oral aspirin therapy)
if visible particles are observed.
SQ: ADULTS, ELDERLY: 1 mg/kg q12h
Administration • Flick syringe so that
the air bubble rises toward the (with oral aspirin).
plunger. • Insert needle subcutaneously STEMI
into abdomen or outer thigh and inject SQ: ADULTS YOUNGER THAN 75 YRS: 30
solution (including air bubble). mg IV once plus 1 mg/kg q12h (maxi-
• Do not inject into areas of active skin mum: 100 mg first 2 doses only). ADULTS
disease or injury such as sunburns, skin 75 YRS OR OLDER: 0.75 mg/kg (maxi-
rashes, inflammation, skin infections, or mum: 75 mg first 2 doses only) q12h.
active psoriasis. • Rotate injection sites.
Storage • Store at room temperature. Acute DVT
SQ: ADULTS, ELDERLY: (inpatient): 1
INDICATIONS/ROUTES/DOSAGE mg/kg q12h or 1.5 mg/kg once daily.
Prevention of Deep Vein Thrombosis (DVT) (outpatient): 1 mg/kg q12h.
After Hip and Knee Surgery
SQ: ADULTS, ELDERLY: Knee surgery: 30 Usual Pediatric Dosage
mg twice daily, generally for 10 days or up SQ: CHILDREN 2 MOS AND OLDER: 0.5 mg/
to 35 days, with initial dose given 12 hrs or kg q12h (prophylaxis); 1 mg/kg q12h (treat-
more pre-operatively or 12 hrs or more ment). NEONATES, INFANTS YOUNGER THAN 2
postoperatively once hemostasis achieved. MOS: 0.75/mg/kg/dose q12h (prophylaxis);
Hip surgery: (Once daily): An initial 1.5 mg/kg/dose q12h (treatment).
dose of 40 mg, given 12 hrs or more pre-
operatively or 12 hrs or more postopera- Dosage in Renal Impairment
tively once hemostasis achieved. Following Elimination is decreased when CrCl is
hip surgery, recommend continuing 40 mg less than 30 mL/min. Monitor and adjust
once daily for at least 10 days or up to 35 dosage as necessary.
days post-op. (Twice daily): 30 mg q12h Use Dosage
with initial dose, 12 hrs or more pre-oper- Abdominal surgery, 30 mg once/day
atively or 12 hrs or more postoperatively pts with acute i­llness
once hemostasis achieved and q12h for at Hip, knee surgery 30 mg once/day
DVT, angina, MI 1 mg/kg once/day
least 10 days or up to 35 days.

Canadian trade name Non-Crushable Drug High Alert drug


424 entecavir
Use Dosage PATIENT/FAMILY TEACHING
STEMI: (younger than 30 mg IV once plus • Usual length of therapy is 7–10 days.
75 yrs) 1 mg/kg q24h • A health care provider will show you
STEMI (75 yrs or 1 mg/kg q24h how to properly prepare and inject your
older)
NSTEMI 1 mg/kg q24h
medication. You must demonstrate correct
preparation and injection techniques be-
Dosage in Hepatic Impairment
fore using medication at home. • Do not
E discontinue current blood thinning regi-
Use caution.
men or take any newly prescribed medica-
SIDE EFFECTS tions unless approved by the prescriber
Occasional (4%–1%): Injection site hema- who originally started treatment. • Sud-
toma, nausea, peripheral edema. denly stopping therapy may i­ncrease the
risk of blood clots or stroke. • Report
ADVERSE EFFECTS/TOXIC bleeding of any kind (bloody urine, stool;
REACTIONS nosebleeds; increased menstrual bleed-
May lead to bleeding complications ing). If bleeding occurs, it may take longer
ranging from local ecchymoses to major to stop bleeding. • Immediately report
hemorrhage. May cause heparin-induced signs of stroke (confusion, headache,
thrombocytopenia (HIT). Antidote: IV numbness, one-sided weakness, trouble
injection of protamine sulfate (1% solu- speaking, loss of vision). • Minor blunt
tion) equal to dose of enoxaparin injected. force trauma to the head, chest, or abdo-
1 mg protamine sulfate neutralizes 1 mg men can be life-threatening. • Do not
enoxaparin. One additional dose of 0.5 take aspirin, herbal supplements, OTC
mg protamine sulfate per 1 mg enoxaparin nonsteroidal anti-inflammatories (may in-
may be given if aPTT tested 2–4 hrs after crease risk of bleeding). • Consult physi-
first injection remains prolonged. cian before any surgery/dental work.
• Use electric razor, soft toothbrush to
NURSING CONSIDERATIONS prevent bleeding.
BASELINE ASSESSMENT
Obtain baseline CBC. Note platelet count.
Question medical history as listed in Pre- entecavir
cautions. Ensure that pt has not received
spinal anesthesia, spinal procedures. As- en-tek-a-veer
sess for active bleeding. Assess pt’s will- (Baraclude, Apo-Entecavir)
ingness to self-inject medication. Assess j BLACK BOX ALERT jSerious,
potential risk of bleeding. sometimes fatal hypersensitivity
reaction, lactic acidosis, severe
INTERVENTION/EVALUATION hepatomegaly with steatosis (fatty
Periodically monitor CBC, platelet count, liver) have occurred. May cause HIV
resistance in chronic hepatitis B pts.
stool for occult blood (no need for daily Severe acute exacerbations of
monitoring in pts with normal presurgical hepatitis B virus infection may occur
coagulation parameters). A decrease in upon discontinuation of entecavir.
the platelet count of more than 50% from
baseline may indicate heparin-induced uCLASSIFICATION
thrombocytopenia. Ensure active hemo- PHARMACOTHERAPEUTIC: Reverse
stasis of puncture site following PCI. As- transcriptase inhibitor, nucleoside.
sess for any sign of bleeding (bleeding at CLINICAL: Antihepadnaviral agent.
surgical site, hematuria, blood in stool,
bleeding from gums, petechiae, bruising,
bleeding from injection sites).

underlined – top prescribed drug


entecavir 425

USES ADMINISTRATION/HANDLING
Treatment of chronic hepatitis B virus PO
(HBV) infection in adults and children • Administer tablets on an empty stom-
2 yrs and older with evidence of active ach (at least 2 hrs after a meal and 2 hrs
viral replication and evidence of either before the next meal). • Do not dilute,
persistent transaminase elevations or mix oral solution with water or any other
histologically active disease or evidence liquid. • Each bottle of oral solution is
of decompensated hepatic disease. OFF- accompanied by a dosing spoon. Before E
LABEL: HBV reinfection prophylaxis, post– administering, hold spoon in vertical po-
liver transplant, HIV/HBV coinfection. sition, fill it gradually to mark corre-
sponding to prescribed dose.
PRECAUTIONS Storage • Store tablets, oral solution
Contraindications: Hypersensitivity to at room temperature.
entecavir. Cautions: Renal impairment,
pts receiving concurrent therapy that INDICATIONS/ROUTES/DOSAGE
may reduce renal function. Pts at risk Chronic Hepatitis B Virus Infection (No
for hepatic disease. Cross resistance may Previous Nucleoside Treatment)
develop with lamivudine. PO: ADULTS, ELDERLY, CHILDREN 16 YRS
AND OLDER: 0.5 mg once daily. CHILDREN 2
ACTION YRS AND OLDER, WEIGHING MORE THAN 30
Inhibits hepatitis B viral polymerase, an KG: 0.5 mg once daily (tablet or solution).
enzyme blocking reverse transcriptase 27–30 KG: 0.45 mg once daily (solution).
activity. Therapeutic Effect: Interferes 24–26 KG: 0.4 mg once daily (solution). 21–
with viral DNA synthesis. 23 KG: 0.35 mg once daily (solution). 18–20
KG: 0.3 mg once daily (solution). 15–17
PHARMACOKINETICS KG: 0.25 mg once daily (solution). 12–14
Poorly absorbed from GI tract. Protein KG: 0.2 mg once daily (solution). 10–11
binding: 13%. Extensively distributed KG: 0.15 mg once daily (solution).
into tissues. Partially metabolized in liver.
Chronic Hepatitis B Virus Infection
Excreted primarily in urine. Half-life: 5–6
(Receiving LamiVUDine, Known
days (increased in renal impairment).
LamiVUDine Resistance, Decompensated
LIFESPAN CONSIDERATIONS Liver Disease)
PO: ADULTS, ELDERLY, CHILDREN 16 YRS AND
Pregnancy/Lactation: Unknown if
OLDER: 1 mg once daily. CHILDREN 2 YRS AND
drug crosses placenta or is distributed in
OLDER, WEIGHING MORE THAN 30 KG: 1 mg
breast milk. Children: Safety and efficacy
not established in pts younger than 16 yrs. once daily (tablet or solution). 27–30 KG: 0.9
Elderly: Age-related renal impairment
mg once daily (solution). 24–26 KG: 0.8 mg
may require dosage adjustment. once daily (solution). 21–23 KG: 0.7 mg once
daily (solution). 18–20 KG: 0.6 mg once daily
INTERACTIONS (solution). 15–17 KG: 0.5 mg once daily (solu-
DRUG: None significant. HERBAL: None tion). 12–14 KG: 0.4 mg once daily (solution).
10–11 KG: 0.3 mg once daily (solution).
significant. FOOD: Food delays absorp-
tion, decreases concentration. LAB VAL- Dosage in Renal Impairment
UES: May increase serum amylase, lipase, Creatinine
bilirubin, ALT, AST, creatinine, glucose. May Clearance Dosage
decrease serum albumin; platelets. 50 mL/min and 0.5 mg once daily
greater
AVAILABILITY (Rx) 30–49 mL/min 0.25 mg once daily
Oral Solution: 0.05 mg/mL. Tablets: 0.5 10–29 mL/min 0.15 mg once daily
mg, 1 mg. 9 mL/min and less 0.05 mg once daily

Canadian trade name Non-Crushable Drug High Alert drug


426 enzalutamide
Dosage in Hepatic Impairment
No dose adjustment. enzalutamide
SIDE EFFECTS en-za-loo-ta-mide
Occasional (4%–3%): Headache, fatigue. (XTANDI)
Rare (less than 1%): Diarrhea, dyspepsia, Do not confuse enzalutamide
nausea, vomiting, dizziness, insomnia. with bicalutamide, flutamide, or
E nilutamide.
ADVERSE EFFECTS/TOXIC
REACTIONS uCLASSIFICATION
Lactic acidosis, severe hepatomegaly with PHARMACOTHERAPEUTIC: An-
steatosis have been reported. Severe, tiandrogen renal inhibitor. CLINI-
acute exacerbations of hepatitis B virus CAL: Antineoplastic.
infection have been reported in pts who
have discontinued therapy; reinitiation of
antihepatitis B therapy may be required. USES
Hematuria occurs occasionally. May Treatment of metastatic castration-resis-
cause development of HIV resistance if tant prostate cancer.
HIV untreated.
PRECAUTIONS
NURSING CONSIDERATIONS Contraindications: Hypersensitivity to
enzalutamide. Women who are pregnant
BASELINE ASSESSMENT
or may become pregnant (not indicated in
Obtain LFT before beginning therapy and female population). Cautions: History of
at periodic intervals during therapy. Offer seizure disorder, underlying brain injury
emotional support. Obtain full medica- with loss of consciousness, transient isch-
tion history. emic attack within past 12 mos, CVA, brain
INTERVENTION/EVALUATION metastases, brain arteriovenous abnor-
mality, use of concurrent medications that
Hepatic function should be monitored
may lower seizure threshold.
closely with both clinical and laboratory
follow-up for at least several mos in pts ACTION
who discontinue antihepatitis B therapy.
Inhibits androgen binding to androgen
For pts on therapy, closely monitor serum
receptors in target tissue, and inhib-
amylase, lipase, bilirubin, ALT, AST, cre-
its interaction with DNA. Therapeutic
atinine, glucose, albumin; platelet count.
Effect: Decreases proliferation, induces
Assess for evidence of GI discomfort.
cell death of prostate cancer cells.
PATIENT/FAMILY TEACHING
PHARMACOKINETICS
• Take medication at least 2 hrs after a
meal and 2 hrs before the next Readily absorbed in GI tract. Maximum
meal. • Avoid transmission of hepatitis plasma concentration achieved in 0.5–3
B infection to others through sexual con- hrs. Metabolized in liver. Protein bind-
tact, blood contamination. • Immedi- ing: (97%–98%). Primarily excreted
ately report unusual muscle pain, ab- in urine. Half-life: 5.8 days (Range:
dominal pain with nausea/vomiting, cold 2.8–10.2 days).
feeling in extremities, dizziness (signs
LIFESPAN CONSIDERATIONS
and symptoms signaling onset of lactic
acidosis). Pregnancy/Lactation: Not used in
female population. Children: Safety and
efficacy not established. Elderly: No
age-related precautions noted.

underlined – top prescribed drug


enzalutamide 427

INTERACTIONS SIDE EFFECTS


DRUG: Strong CYP2C8, CYP3A4 Common (51%): Asthenia. Frequent (26%–
inhibitors (e.g., gemfibrozil, itra- 15%): Back pain, diarrhea, arthralgia, hot
conazole) may increase concentration/ flashes, peripheral edema, musculoskeletal
effect. CYP3A4 inducers (e.g., car- pain. Occasional (12%–6%): Headache, diz-
BAMazepine, phenytoin, rifAMPin) ziness, insomnia, hematuria, paresthesia,
may decrease concentration/effect. anxiety, hypertension. Rare (4%–2%): Men-
May decrease concentration/effect of tal impairment disorders (includes E
cycloSPORINE, ergot derivatives amnesia, memory impairment, cognitive
(e.g., ergotamine), fosphenytoin, disorder, attention deficit), hematuria
phenytoin, sirolimus, tacrolimus. (includes pollakiuria, pruritus, dry skin).
HERBAL: St. John’s wort may decrease
concentration/effect. FOOD: None ADVERSE EFFECTS/TOXIC
known. LAB VALUES: May increase REACTIONS
serum ALT, AST, bilirubin. May decrease Upper respiratory tract infection occurs
Hgb, Hct, platelets, WBC count. in 11% of pts; lower respiratory tract
and lung infection (includes pneumonia,
AVAILABILITY (Rx) bronchitis) occur in slightly less (9% of
Capsules: 40 mg. pts). Spinal cord compression and cauda
equina syndrome occur in 7% of pts.
ADMINISTRATION/HANDLING
PO
NURSING CONSIDERATIONS
• May give with or without food. Take at BASELINE ASSESSMENT
same time each day. Swallow Offer emotional support. Obtain LFT at
whole. • Do not break, crush, dissolve, baseline and periodically throughout
or open capsules. therapy. Assess bowel activity, stool con-
INDICATIONS/ROUTES/ sistency. If coadministered with warfarin
DOSAGE (CYP2C9 substrate), perform additional
INR monitoring.
Metastatic Castration-Resistant Prostate
Cancer INTERVENTION/EVALUATION
PO: ADULTS, ELDERLY: 160 mg (4 × 40 Assess for peripheral edema. Question
mg capsules) given once daily. level of fatigue, weakness. Question pres-
ence of back pain, arthralgia, or head-
Dose Modification ache. Assess level of anxiety. Monitor B/P
If CTCAE Grade 3 or greater toxicity or an for hypertension. Assess for hematuria.
intolerable side effect occurs, withhold Question pt regarding sleeping pattern.
dosing for 1 week or until symptoms
improve to Grade 2 or less, then resume PATIENT/FAMILY TEACHING
at same dose or a reduced dose (120 mg • Sexually active men must wear con-
or 80 mg). Concurrent use of strong dom during treatment and for 1 wk after
CYP2C8 inhibitors: Avoid use (if pos- treatment due to potential risks to fe-
sible). If concurrent use is necessary, tus. • Women who are pregnant or are
reduce the enzalutamide dose to 80 mg planning pregnancy may not touch medi-
once daily. Concurrent use of strong cation without gloves. • Dizziness,
CYP3A4 inducers: Increase dose to headache, muscle weakness, leg swell-
240 mg once daily. ing/discomfort should be reported.
• Immediately report fever or
Dosage in Renal/Hepatic Impairment cough. • Routine lab testing will occur
No dose adjustment. during treatment.

Canadian trade name Non-Crushable Drug High Alert drug


428 EPINEPHrine
of tricyclic antidepressants. History of
EPINEPHrine prostate enlargement, urinary retention.
ep-i-nef-rin ACTION
(Adrenalin, EpiPen, EpiPen Jr., Stimulates alpha-adrenergic receptors
Twinject ) (vasoconstriction, pressor effects), beta1-
Do not confuse EPINEPHrine adrenergic receptors (cardiac stimula-
E with ePHEDrine. tion), beta2-adrenergic receptors (bron-
chial dilation, vasodilation). Therapeutic
FIXED-COMBINATION(S) Effect: Relaxes smooth muscle of bron-
LidoSite: EPINEPHrine/lidocaine (an- chial tree, produces cardiac stimulation,
esthetic): 0.1%/10%. dilates skeletal muscle vasculature.
uCLASSIFICATION PHARMACOKINETICS
PHARMACOTHERAPEUTIC: Sympa- Route Onset Peak Duration
thomimetic (alpha-, beta-adrenergic IM 5–10 min 20 min 1–4 hrs
agonist). CLINICAL: Antiglaucoma, SQ 5–10 min 20 min 1–4 hrs
bronchodilator, cardiac stimulant, Inhalation 3–5 min 20 min 1–3 hrs
antiallergic, antihemorrhagic, pria-
pism reversal agent. Well absorbed after parenteral admin-
istration; minimally absorbed after
inhalation. Metabolized in liver, other
USES tissues, sympathetic nerve endings.
Treatment of allergic reactions (includ- Excreted in urine. Ophthalmic form
ing anaphylactic reactions). Treatment of may be systemically absorbed as a
hypotension associated with septic shock. result of drainage into nasal pharyn-
Added to local anesthetics to decrease geal passages. Mydriasis occurs within
systemic absorption and increase dura- several min and persists several hrs;
tion of activity of local anesthetic. vasoconstriction occurs within 5 min
Decreases superficial hemorrhage. OFF- and lasts less than 1 hr.
LABEL: Ventricular fibrillation or pulse-
less ventricular tachycardia unresponsive LIFESPAN CONSIDERATIONS
to initial defibrillatory shocks; pulseless Pregnancy/Lactation: Crosses placenta.
electrical activity, asystole, hypotension Distributed in breast milk. Children/
unresponsive to volume resuscitation; Elderly: No age-related precautions
bradycardia/hypotension unresponsive noted.
to atropine or pacing; inotropic support.
INTERACTIONS
PRECAUTIONS DRUG: May decrease effects of beta
Contraindications: Hypersensitivity to blockers (e.g., carvedilol, metopro-
EPINEPHrine. Note: There are no ab­­ lol). Digoxin, sympathomimetics
solute contraindications with inject- (e.g., dopamine, norepinephrine)
able EPINEPHrine in a life-threatening may increase risk of arrhythmias.
situation. IV: Narrow-angle glaucoma, Ergonovine, methergine, oxytocin
thyrotoxicosis, diabetes, hypertension, may increase vasoconstriction. MAOIs
other cardiovascular disorders. Inhala- (e.g., phenelzine, selegiline), tri-
tion: Concurrent use or within 2 wks cyclic antidepressants (e.g., ami-
of MAOIs. Cautions: Elderly, diabetes triptyline, doxepin, nortriptyline)
mellitus, hypertension, Parkinson’s dis- may increase cardiovascular effects.
ease, thyroid disease, cerebrovascular or HERBAL: Ephedra, yohimbe may
cardiovascular disease, concurrent use increase CNS stimulation. FOOD: None

underlined – top prescribed drug


EPINEPHrine 429
known. LAB VALUES: May decrease IV INCOMPATIBILITIES
serum potassium. Ampicillin, pantoprazole (Protonix),
sodium bicarbonate.
AVAILABILITY (RX)
Injection, Solution (Prefilled Syringes): IV COMPATIBILITIES
(EpiPen): 0.3 mg/0.3 mL. (EpiPen Calcium chloride, calcium gluconate,
Jr.): 0.15 mg/0.3 mL. (Twinject): 0.15 dexmedetomidine (Precedex), dilTIA-
mg/0.15 mL. Injection, Solution: 0.1 mg/ Zem (Cardizem), DOBUTamine (Dobu- E
mL (1:10,000), 1 mg/mL (1:1,000). trex), DOPamine (Intropin), fentaNYL
(Sublimaze), heparin, HYDROmorphone
Solution for Oral Inhalation: (Adrenalin):
(Dilaudid), LORazepam (Ativan), mid-
2.25% (0.5 mL). azolam (Versed), milrinone (Primacor),
ADMINISTRATION/HANDLING morphine, nitroglycerin, norepinephrine
(Levophed), potassium chloride, propofol
IV (Diprivan).
Reconstitution • For injection, dilute INDICATIONS/ROUTES/DOSAGE
each 1 mg of 1:1,000 solution with 10 mL
Anaphylaxis
0.9% NaCl to provide 1:10,000 solution
IM, SQ: ADULTS, ELDERLY: 0.2–0.5 mg
and inject each 1 mg or fraction thereof
(0.2–0.5 mL of 1:1,000 solution). May
over 1 min or more (except in cardiac
repeat q5–15 min if anaphylaxis persists.
arrest). • For infusion, further dilute
CHILDREN: 0.01 mg/kg (0.01 mL/kg of
with 250–500 mL D5W. Maximum con-
a 1:1,000 solution) q5–15 min. Maxi-
centration 64 mcg/mL.
mum: 0.3–0.5 mg q5–15 min.
Rate of administration • For IV infu-
sion, give at 1–10 mcg/min (titrate to Hypotension (Shock)
desired response). IV infusion: ADULTS, ELDERLY: Initially,
Storage • Store parenteral forms at 0.1-0.5 mcg/kg/min. Titrate to desired
room temperature. • Do not use if so- response.
lution appears discolored or contains a
precipitate. Cardiac Arrest
IV: ADULTS, ELDERLY: Initially, 1 mg.
SQ May repeat q3–5min as needed. CHIL-
• Shake ampule thoroughly. • Use tu- DREN: Initially, 0.01 mg/kg (0.1 mL/
berculin syringe for injection into lateral kg of a 1:10,000 solution). May repeat
deltoid region. • Massage injection site q3–5min as needed.
(minimizes vasoconstriction effect). Use Endotracheal: ADULTS, ELDERLY: 2–2.5
only 1:1,000 solution. mg q3–5 min as needed. CHILDREN: 0.1
mg/kg (0.1 mL/kg of a 1:1,000 solution).
Nebulizer
May repeat q3–5min as needed. Maxi-
• No more than 10 drops Adrenalin Chlo-
mum single dose: 2.5 mg.
ride solution 1:100 should be placed in
reservoir of nebulizer. • Place nozzle just Dosage in Renal/Hepatic Impairment
inside pt’s partially opened mouth. • As No dose adjustment.
bulb is squeezed once or twice, instruct pt
to inhale deeply, drawing vaporized solution SIDE EFFECTS
into lungs. • Rinse mouth with water im- Frequent: Systemic: Tachycardia, pal-
mediately after inhalation (prevents mouth/ pitations, anxiety. Ophthalmic: Head-
throat dryness). • When nebulizer is not ache, eye irritation, watering of eyes.
in use, replace stopper, keep in upright Occasional: Systemic: Dizziness, light-
position. headedness, facial flushing, headache,

Canadian trade name Non-Crushable Drug High Alert drug


430 eplerenone
diaphoresis, increased B/P, nausea, trem- PRECAUTIONS
bling, insomnia, vomiting, fatigue. Oph- Contraindications: Hypersensitivity to
thalmic: Blurred/decreased vision, eye eplerenone. Concurrent use with strong
pain. Rare: Systemic: Chest discomfort/ CYP3A4 inhibitors (e.g., ketoconazole,
pain, arrhythmias, bronchospasm, dry itraconazole), CrCl less than 30 mL/
mouth/throat. min, serum potassium level greater
than 5.5 mEq/L at initiation. Use in pts
E ADVERSE EFFECTS/TOXIC
with Addison’s disease. Hypertension
REACTIONS
(Additional): Type 2 diabetes with
Excessive doses may cause acute hyper- microalbuminuria; CrCl less than 50
tension, arrhythmias. Prolonged/exces- mL/min; serum creatinine greater than
sive use may result in metabolic acidosis 2 mg/dL in men, greater than 1.8 mg/dL
due to increased serum lactic acid. Meta- in women; concomitant use of potassium
bolic acidosis may cause disorientation, supplements or potassium-sparing diuret-
fatigue, hyperventilation, headache, nau- ics. Cautions: Hyperkalemia, HF, post-MI,
sea, vomiting, diarrhea. diabetes, mild renal impairment.
NURSING CONSIDERATIONS ACTION
INTERVENTION/EVALUATION Binds to mineralocorticoid receptors
Monitor changes of B/P, HR. Assess lung in kidney, heart, blood vessels, brain,
sounds for rhonchi, wheezing, rales. blocking binding of aldosterone. Thera-
Monitor ABGs. In cardiac arrest, adhere peutic Effect: Reduces B/P. Prevents
to ACLS protocols. myocardial and vascular fibrosis.
PATIENT/FAMILY TEACHING PHARMACOKINETICS
• Avoid excessive use of caffeine. • Re- Absorption unaffected by food. Pro-
port any new symptoms (tachycardia, tein binding: 50%. Metabolized in liver.
shortness of breath, dizziness) immedi- Excreted in urine (67%), feces (32%).
ately: may be systemic effects. Not removed by hemodialysis. Half-
life: 4–6 hrs.
LIFESPAN CONSIDERATIONS
eplerenone Pregnancy/Lactation: Unknown if
drug crosses placenta or is distributed
ep-ler-e-none in breast milk. Children: Safety and effi-
(Inspra) cacy not established. Elderly: No age-
Do not confuse Inspra with related precautions noted.
Spiriva.
INTERACTIONS
uCLASSIFICATION DRUG: ACE inhibitors (e.g., enala-
PHARMACOTHERAPEUTIC: Aldos- pril, lisinopril), angiotensin II
terone receptor antagonist. CLINI- antagonists (e.g., losartan, valsar-
CAL: Antihypertensive. tan), potassium-sparing diuretics
(e.g., spironolactone), potassium
supplements increase risk of hyperka-
USES lemia. May increase the hyperkalemic
Treatment of hypertension alone or in effect of cycloSPORINE, tacrolimus.
combination with other antihypertensive Strong CYP3A4 inhibitors (e.g.,
agents. Treatment of HF following acute clarithromycin, ketoconazole,
myocardial infarction (AMI). ritonavir) may increase concentra-
tion/effect. Strong CYP3A4 inducers
underlined – top prescribed drug
eplerenone 431
(e.g., carBAMazepine, phenytoin, Dosage in Renal Impairment
rifAMPin) may decrease concentration/ Contraindicated in pts with hypertension
effect. NSAIDs may decrease antihyper- with CrCl less than 50 mL/min or serum
tensive effect. HERBAL: None signifi- creatinine greater than 2 mg/dL in males
cant. FOOD: Grapefruit products may or greater than 1.8 mg/dL in females. All
increase potential for hyperkalemia, other indications, CrCl less than 30 mL/
arrhythmias. LAB VALUES: May increase min, use is contraindicated.
serum potassium, ALT, AST, cholesterol, E
triglycerides, serum creatinine, uric acid. Dosage in Hepatic Impairment
May decrease serum sodium. No dose adjustment.

AVAILABILITY (Rx) SIDE EFFECTS


Rare (3%–1%): Dizziness, diarrhea,
Tablets: 25 mg, 50 mg. cough, fatigue, flu-like symptoms,
ADMINISTRATION/HANDLING abdominal pain.
• Do not break, crush, dissolve, or di- ADVERSE EFFECTS/TOXIC
vide film-coated tablets. • May give REACTIONS
without regard to food. Hyperkalemia may occur, particularly
INDICATIONS/ROUTES/DOSAGE in pts with type 2 diabetes mellitus and
microalbuminuria.
Hypertension
PO: ADULTS, ELDERLY: Initially, 50 mg NURSING CONSIDERATIONS
once daily. If 50 mg once daily pro-
duces an inadequate B/P response, may BASELINE ASSESSMENT
increase dosage to 50 mg twice daily. If pt Obtain serum potassium level. Obtain
is concurrently receiving CYP3A4 inhibi- B/P, apical pulse immediately before
tors (e.g., erythromycin, verapamil, or each dose, in addition to regular
fluconazole), reduce initial dose to 25 monitoring (be alert to fluctuations).
mg once daily. Maximum: 50 mg/day. If excessive reduction in B/P occurs,
place pt in supine position, feet slightly
HF Following MI elevated.
PO: ADULTS, ELDERLY: Initially, 25 mg
once daily. If tolerated, titrate up to 50 INTERVENTION/EVALUATION
mg once daily within 4 wks. Assist with ambulation if dizziness oc-
curs. Monitor serum potassium levels.
Dosage Adjustment for Serum Potassium Assess B/P for hypertension/hypotension.
Concentrations in HF Monitor daily pattern of bowel activity,
Less than 5 mEq/L: Increase dose stool consistency. Assess for evidence of
from 25 mg daily to 50 mg daily or flu-like symptoms.
increase dose from 25 mg every other
day to 25 mg daily. 5–5.4 mEq/L: PATIENT/FAMILY TEACHING
No adjustment needed. 5.5–5.9 mEq/L: • Avoid tasks that require alertness,
Decrease dose from 50 mg daily to 25 motor skills until response to drug is
mg daily or from 25 mg daily to 25 mg established (possible dizziness ef-
every other day. Decrease dose from 25 fect). • Hypertension requires lifelong
mg every other day to withhold medica- control. • Avoid exercising during hot
tion. 6 mEq/L or greater: Withhold weather (risk of dehydration, hypoten-
medication until potassium is less than sion). • Do not use salt substitutes
5.5 mEq/L, then restart at 25 mg every containing potassium.
other day.

Canadian trade name Non-Crushable Drug High Alert drug


432 epoetin alfa
achieved with epoetin alfa. Chronic renal
epoetin alfa failure pts: Increased risk for serious
cardiovascular reactions (e.g., stroke, MI)
e-poe-e-tin al-fa when Hgb levels greater than 11 g/dL are
(Epogen, Eprex , Procrit) achieved with epoetin alfa.
j BLACK BOX ALERT j Increased
risk of serious cardiovascular ACTION
E events, thromboembolic events,
mortality, time-to-tumor progression Stimulates division, differentiation of ery-
in pts with head and neck cancer, throid progenitor cells in bone marrow.
metastatic breast cancer, non– Therapeutic Effect: Induces erythro-
small-cell lung cancer when admin- poiesis, releases reticulocytes from bone
istered to a target hemoglobin of marrow into blood, where they mature
more than 11 g/dL. Increases rate of
deep vein thrombosis in periopera- into erythrocytes.
tive pts not receiving anticoagulant
therapy. PHARMACOKINETICS
Do not confuse epoetin with Well absorbed after SQ administration.
darbepoetin, or Epogen with Following administration, an increase
Neupogen. in reticulocyte count occurs within 10
days, and increases in Hgb, Hct, and RBC
uCLASSIFICATION count are seen within 2–6 wks. Half-
PHARMACOTHERAPEUTIC: Eryth- life: 4–13 hrs.
ropoiesis-stimulating agent (ESA).
CLINICAL: Erythropoietin. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if
drug crosses placenta or is distributed
USES in breast milk. Children: Safety and
Treatment of anemia in pts receiving efficacy not established in pts 12 yrs and
or who have received myelosuppres- younger. Elderly: No age-related pre-
sive chemotherapy for a planned mini- cautions noted.
mum of 2 mos of chemotherapy; pts
with chronic renal failure to decrease INTERACTIONS
need for RBC transfusion; HIV-infected DRUG: None significant. HERBAL: None
pts on zidovudine (AZT) therapy when significant. FOOD: None known. LAB
endogenous erythropoietin levels are VALUES: May increase serum BUN,
500 Units/mL or less; pts scheduled for phosphorus, potassium, creatinine, uric
elective noncardiac, nonvascular sur- acid, sodium. May decrease bleeding
gery, reducing need for allogenic blood time, iron concentration, serum ferritin.
transfusions when perioperative Hgb is
greater than 10 or less than or equal AVAILABILITY (Rx)
to 13 g/dL and high risk for blood loss. Injection Solution: (Epogen, Pro-
OFF-LABEL: Anemia in myelodysplastic crit): 2,000 units/mL, 3,000 units/mL,
syndromes. 4,000 units/mL, 10,000 units/mL, 20,000
units/mL, 40,000 units/mL.
PRECAUTIONS
Contraindications: Hypersensitivity to ADMINISTRATION/HANDLING
epoetin. Pure red cell aplasia that begins b ALERT c Avoid excessive agitation of
after treatment, uncontrolled hyperten- vial; do not shake (foaming).
sion. Cautions: History of seizures or con- IV
trolled hypertension. Cancer pts: Tumor
growth, shortened survival may occur Reconstitution • No reconstitution
when Hgb levels of 11 g/dL or greater are necessary.

underlined – top prescribed drug


epoetin alfa 433
Rate of administration • May be gery or 600 units/kg once weekly for 4
given as an IV bolus. doses given 21, 14, 7 days before surgery
Storage • Refrigerate. • Vigorous and on the day of surgery.
shaking may denature medication, ren-
dering it inactive. Anemia in Chronic Renal Failure
b ALERT c Individualize dose, using
SQ lowest dose to reduce need for RBC
• Mix in syringe with bacteriostatic 0.9% transfusions. ON DIALYSIS: Initiate E
NaCl with benzyl alcohol 0.9% (bacterio- when Hgb less than 10 g/dL; reduce dose
static saline) at a 1:1 ratio (benzyl alcohol or discontinue if Hgb approaches or ex-
acts as local anesthetic; may reduce injection ceeds 11 g/dL. NOT ON DIALYSIS: Ini-
site discomfort). • Use 1 dose per vial; do tiate when Hgb less than 10 g/dL; reduce
not reenter vial. Discard unused portion. dose or stop if Hgb exceeds 10 g/dL.
IV, SQ: ADULTS, ELDERLY: 50–100
IV INCOMPATIBILITIES units/kg 3 times/wk. CHILDREN: 50 units/
Do not mix injection form with other kg 3 times/wk. Maintenance: Decrease
medications. dose by 25%: If Hgb increases greater
INDICATIONS/ROUTES/DOSAGE than 1 g/dL in any 2-wk period. Increase
dose by 25%: If Hgb does not increase
Anemia Associated with Chemotherapy
by greater than 1 g/dL after 4 wks of
b ALERT c Begin therapy only if Hgb less
therapy. Do not increase dose more fre-
than 10 g/dL and anticipated duration of quently than every 4 wks. Note: If pt does
myelosuppressive chemotherapy is greater not attain adequate response after appropri-
than 2 mos. Use minimum effective dose to ate dosing over 12 wks, do not continue to
maintain Hgb level that will avoid red increase dose, and use minimum effective
blood cell transfusions. Discontinue upon dose to maintain Hgb level that will avoid red
completion of chemotherapy. blood cell transfusions.
SQ: ADULTS, ELDERLY: Initially, 150
units/kg 3 times/wk (commonly used HIV Infection in Pts Treated with
dose of 10,000 units 3 times/wk) or Zidovudine (AZT)
40,000 units once wkly. IV: CHILDREN 5 IV, SQ: ADULTS: Initially, 100 units/
YRS AND OLDER: 600 units/kg once wkly. kg 3 times/wk for 8 wks; may increase
Maximum: 40,000 units. by 50–100 units/kg 3 times/wk. Evalu-
Increase dose: ADULTS, ELDERLY: If Hgb ate response q4–8wks thereafter. Adjust
does not increase by greater than 1 g/dL dosage by 50–100 units/kg 3 times/wk. If
and remains below 10 g/dL after initial dosages larger than 300 units/kg 3 times/
4 wks, may increase to 300 units/kg 3 wk are not eliciting response, it is unlikely
times/wk or 60,000 units once wkly. CHIL- pt will respond. Maintenance: Titrate to
DREN: If Hgb does not increase by greater maintain desired Hgb level. Hgb levels
than 1 g/dL and remains less than 10 g/ should not exceed 12 g/dL. If Hgb greater
dL after initial 4 wks of once-wkly dosing, than 12 g/dL, resume treatment with 25%
may increase dose to 900 units/kg/wk. dose reduction when Hgb drops below
Maximum: 60,000 units once wkly. 11 g/dL. Discontinue if Hgb increase not
Decrease dose: Decrease dose by 25% attained with 300 units/kg for 8 wks.
if Hgb increases greater than 1 g/dL in any
2-wk period or Hgb level reaches level Dosage in Renal/Hepatic Impairment
that will avoid red blood cell transfusions. No dose adjustment.

Reduction of Allogenic Blood SIDE EFFECTS


Transfusions in Elective Surgery Pts Receiving Chemotherapy
SQ: ADULTS, ELDERLY: 300 units/kg/day Frequent (20%–17%): Fever, diarrhea, nau-
for 10 days before and 4 days after sur- sea, vomiting, edema. Occasional (13%–
Canadian trade name Non-Crushable Drug High Alert drug
434 eprosartan
11%): Asthenia, shortness of breath, pares- PATIENT/FAMILY TEACHING
thesia. Rare (5%–3%): Dizziness, trunk pain. • Frequent laboratory assessments
needed to determine correct dos-
Pts with Chronic Renal Failure age. • Immediately report any severe
Frequent (24%–11%): Hypertension, head- headache. • Avoid potentially hazard-
ache, nausea, arthralgia. Occasional (9%– ous activity during first 90 days of therapy
7%): Fatigue, edema, diarrhea, vomiting, (increased risk of seizures in pts with
E chest pain, skin reactions at administra- chronic renal failure during first 90
tion site, asthenia, dizziness. days). • Specific dietary regimen must
Pts with HIV Infection Treated with AZT
be maintained.
Frequent (38%–15%): Fever, fatigue,
headache, cough, diarrhea, rash, nau-
sea. Occasional (14%–9%): Shortness of
breath, asthenia, skin reaction at injec- eprosartan
tion site, dizziness.
ep-roe-sar-tan
ADVERSE EFFECTS/TOXIC (Teveten)
REACTIONS j BLACK BOX ALERT jMay
cause fetal injury, mortality. Dis-
Hypertensive encephalopathy, throm- continue as soon as possible once
bosis, cerebrovascular accident, MI, pregnancy is detected.
seizures occur rarely. Hyperkalemia
occurs occasionally in pts with chronic FIXED-COMBINATION(S)
renal failure, usually in those who do not Teveten HCT: eprosartan/hydro-
comply with medication regimen, dietary CHLOROthiazide (a diuretic): 400
guidelines, frequency of dialysis regimen. mg/12.5 mg.
NURSING CONSIDERATIONS uCLASSIFICATION
BASELINE ASSESSMENT PHARMACOTHERAPEUTIC: Angio-
Assess B/P before initiation (80% of pts tensin II receptor antagonist. CLINI-
CAL: Antihypertensive.
with chronic renal failure have history
of hypertension). B/P often rises dur-
ing early therapy in pts with history of USES
hypertension. Consider that all pts even- Treatment of hypertension (alone or in
tually need supplemental iron therapy. combination with other medications).
Assess serum iron (should be greater
than 20%), serum ferritin (should be PRECAUTIONS
greater than 100 ng/mL) before and dur- Contraindications: Hypersensitivity
ing therapy. Establish baseline CBC (esp. to eprosartan. Concomitant use with
note Hct). aliskiren in pts with diabetes. Cau-
INTERVENTION/EVALUATION tions: Unstented unilateral/bilateral
renal artery stenosis, preexisting renal
Assess CBC routinely (esp. Hgb, Hct). insufficiency. Concomitant use of potas-
Monitor aggressively for increased B/P sium-sparing medications (e.g., spirono-
(25% of pts require antihypertensive lactone), potassium supplements, pts
therapy, dietary restrictions). Monitor who are volume depleted.
temperature, esp. in cancer pts on che-
motherapy and zidovudine-treated HIV ACTION
pts. Monitor serum BUN, uric acid, cre- Potent vasodilator. Blocks vasocon-
atinine, phosphorus, potassium, esp. in strictor, aldosterone-secreting effects
chronic renal failure pts. of angiotensin II, inhibiting binding
underlined – top prescribed drug
eprosartan 435
of angiotensin II to AT1 receptors. Dosage in Renal Impairment
Therapeutic Effect: Causes vasodila- Mild impairment: No dose adjust-
tion, decreases peripheral resistance, ment. Moderate to severe impair-
decreases B/P. ment: Maximum: 600 mg/day.

PHARMACOKINETICS Dosage in Hepatic Impairment


Rapidly absorbed after PO adminis- No dose adjustment. Severe impair-
tration. Protein binding: 98%. Mini- ment: Maximum: 600 mg/day. E
mally metabolized in liver. Primarily SIDE EFFECTS
excreted via urine, biliary system. Mini-
mally removed by hemodialysis. Half- Occasional (5%–2%): Headache, cough,
life: 5–9 hrs. dizziness. Rare (less than 2%): Muscle
pain, fatigue, diarrhea, upper respiratory
LIFESPAN CONSIDERATIONS tract infection, dyspepsia.
Pregnancy/Lactation: Has caused ADVERSE EFFECTS/TOXIC
fetal and neonatal morbidity and mor- REACTIONS
tality. Potential for adverse effects on
breastfeeding infant. Breastfeeding not Overdosage may manifest as hypoten-
recommended. Children: Safety and sion, tachycardia. Bradycardia occurs
efficacy not established. Elderly: No less often.
age-related precautions noted. NURSING CONSIDERATIONS
INTERACTIONS BASELINE ASSESSMENT
DRUG: Aliskiren may increase hyper- Obtain B/P, apical pulse immediately
kalemic effect. May increase adverse/ before each dose, in addition to regular
toxicity of ACE inhibitors (e.g., bena- monitoring (be alert to fluctuations).
zepril, lisinopril). HERBAL: Herbals Question for possibility of pregnancy, his-
with hypertensive properties (e.g., tory of hepatic/renal impairment, renal
licorice, yohimbe) or hypoten- artery stenosis. Obtain urine pregnancy
sive properties (e.g., garlic, gin- test. Assess medication history (esp. di-
ger, ginkgo biloba) may alter effects. uretics).
FOOD: None known. LAB VALUES: May
increase serum BUN, alkaline phospha- INTERVENTION/EVALUATION
tase, bilirubin, creatinine, ALT, AST. May Monitor B/P, pulse, serum BUN, creati-
decrease Hgb, Hct. nine, electrolytes, urinalysis.
AVAILABILITY (Rx) PATIENT/FAMILY TEACHING

Tablets: 400 mg, 600 mg. • Inform female pt regarding conse-


quences of second- and third-trimes-
ADMINISTRATION/HANDLING ter exposure to medication. • Avoid
PO
tasks that require alertness, motor
• Give without regard to food. • Do skills until response to drug is estab-
not break, crush, dissolve, or divide tab- lished. • Restrict sodium, alcohol
lets. intake. • Follow diet, control
weight. • Do not stop taking medica-
INDICATIONS/ROUTES/DOSAGE tion; hypertension requires lifelong
Hypertension
control. • Check B/P regu-
PO: ADULTS, ELDERLY: Initially, 600 mg larly. • Do not chew, crush, dissolve,
once daily. Titrate up to 800 mg/day in or divide tablets; take whole.
1-2 divided doses.

Canadian trade name Non-Crushable Drug High Alert drug


436 eptifibatide

eptifibatide PHARMACOKINETICS
Protein binding: 25%. Excreted in urine.
ep-ti-fye-ba-tide Half-life: 2.5 hrs.
(Integrilin)
INTERACTIONS
uCLASSIFICATION DRUG: Antiplatelets (e.g., aspirin,
E PHARMACOTHERAPEUTIC: Glyco- clopidogrel, prasugrel, ticagrelor)
protein IIb/IIIa inhibitor. CLINI- may increase anticoagulant effect; risk of
CAL: Antiplatelet. ­bleeding. HERBAL: Herbals with antico-
agulant/antiplatelet activity (e.g., gar-
lic, ginger, ginkgo biloba) may increase
USES adverse effects. FOOD: None known. LAB
Treatment of pts with acute coronary VALUES: Increases PT, aPTT. Decreases
syndrome (ACS), including those man- platelet count. Prolongs clotting time.
aged medically and those undergoing
percutaneous coronary intervention AVAILABILITY (Rx)
(PCI). Treatment of pts undergoing PCI, Injection Solution: 0.75 mg/mL, 2 mg/mL.
including intracoronary stenting. OFF-
LABEL: Support PCI during ST-elevation
ADMINISTRATION/HANDLING
myocardial infarction (STEMI). IV

PRECAUTIONS Reconstitution • Withdraw bolus


dose from 10-mL vial (2 mg/mL); for IV
Contraindications: Hypersensitivity to
infusion, withdraw from 100-mL vial
eptifibatide. Active abnormal b­leeding
(0.75 mg/mL). • IV push and infusion
within previous 30 days; history of bleeding
administration may be given undiluted.
diathesis; history of stroke within 30 days
Rate of administration • Give bolus
or history of hemorrhagic stroke; severe
dose IV push over 1–2 min.
hypertension (systolic B/P greater than
Storage • Store vials in refrigera-
200 mm Hg or diastolic B/P greater than
tor. • Solution appears clear, color-
110 mm Hg); major surgery within previ-
less. • Do not shake. • Discard any
ous 6 wks; dependency on hemodialysis.
unused portion left in vial; discard if
Cautions: Renal impairment, hemorrhagic
preparation contains any opaque particles.
retinopathy, platelet count less than 100,000
cells/mm3, elderly, history of bleeding disor- IV INCOMPATIBILITIES
der. Medications that increase risk of bleed-
Administer via dedicated line; do not add
ing (e.g., oral anticoagulants, antiplatelets).
other medications to infusion solution.
ACTION IV COMPATIBILITIES
Blocks platelet glycoprotein IIb/IIIa
Amiodarone (Cordarone), argatroban,
receptor (binding site for fibrinogen,
bivalirudin, metoprolol (Lopressor).
von Willebrand factor). Therapeutic
Effect: Prevents thrombus formation INDICATIONS/ROUTES/DOSAGE
within coronary arteries. Prevents plate-
Adjunct to Percutaneous Coronary
let aggregation.
Intervention (PCI) (With or without
LIFESPAN CONSIDERATIONS Stenting)
IV bolus, IV infusion: ADULTS,
Pregnancy/Lactation: Unknown if
ELDERLY: 180 mcg/kg (maximum: 22.6
excreted in breast milk. Children/
mg) before PCI initiation; then continuous
Elderly: No age-related precautions
drip of 2 mcg/kg/min and a second 180
noted.
mcg/kg (maximum: 22.6 mg) bolus 10
underlined – top prescribed drug
erdafitinib 437
min after the first. Maximum: 15 mg/hr.
May continue infusion for 2-24 hrs after erdafitinib
PCI. Concurrent aspirin and heparin ther-
apy is recommended. er-da-fi-ti-nib
(Balversa)
Acute Coronary Syndrome (ACS) Do not confuse erdafitinib
IV bolus, IV infusion: ADULTS, with enasidenib, encorafenib,
ELDERLY: 180 mcg/kg over 1–2 min erlotinib or gefitinib, or Balvera E
(maximum: 22.6 mg) bolus then 2 with Balziva.
mcg/kg/min continuous infusion (Maxi-
mum 15 mg/hr); a second bolus of 180 uCLASSIFICATION
mcg/kg (maximum 22.6 mg) given 10 PHARMACOTHERAPEUTIC: Fibro-
min after first bolus. May continue infu- blast growth factor receptor (FGFR)
sion up to 18-24 hrs after PCI. Maxi- inhibitor. Tyrosine kinase inhibitor.
mum: 15 mg/hr. Concurrent aspirin and CLINICAL: Antineoplastic.
heparin therapy is recommended.
Dosage in Renal Impairment
CrCl less than 50 mL/min: Use 180 USES
mcg/kg bolus (maximum: 22.6 mg) Treatment of adult pts with locally ad-
and 1 mcg/kg/min infusion (maximum: vanced or metastatic urothelial carci-
7.5 mg/hr). End-stage renal disease noma that has susceptible FGFR3 or
(dialysis): Contraindicated. FGFR2 genetic mutation alterations and
progressed during or following at least
Dosage in Hepatic Impairment one line of prior platinum-containing
No dose adjustment. chemotherapy including within 12 mos
of neoadjuvant or adjuvant platinum-
SIDE EFFECTS containing chemotherapy.
Occasional (7%): Hypotension.
PRECAUTIONS
ADVERSE EFFECTS/TOXIC
Contraindications: Hypersensitivity to
REACTIONS
erdafitinib. Cautions: Baseline hemo-
Minor to major bleeding complications globinemia, neutropenia, leukopenia,
may occur, most commonly at arterial thrombocytopenia; conditions pre-
access site for cardiac catheterization. disposing to infection (e.g., diabetes,
NURSING CONSIDERATIONS renal failure, immunocompromised
pts, open wounds), hepatic/renal
BASELINE ASSESSMENT impairment, optic disorders, pts at
Assess platelet count, Hgb, Hct before risk for hyperphosphatemia (hypo-
treatment and during therapy. If platelet parathyroidism, concomitant use of
count less than 90,000 cells/mm3, addi- phosphorus-containing medications,
tional platelet counts should be obtained chronic kidney disease), CYP2C9 poor
routinely to avoid thrombocytopenia. metabolizers (pts with CYP2C9*3/*3
genotype); concomitant use of CYP3A
INTERVENTION/EVALUATION inhibitors or inducers, CYP2C9 induc-
Diligently monitor for potential bleed- ers or inhibitors, CYP34A substrates,
ing, particularly at other arterial, venous OAT2 substrates, or P-gp substrates.
puncture sites. If possible, urinary cathe-
ters, nasogastric tubes should be avoided.

Canadian trade name Non-Crushable Drug High Alert drug


438 erdafitinib

ACTION HERBAL: St. John’s wort may decrease


Binds to and inhibits fibroblast growth concentration/effect. FOOD: Phospho-
factor receptor (FGFR) enzyme activity. rus-containing foods (e.g., dairy
Decreases FGFR-related signaling and products, deli meats, nuts, peanut
cell viability. Therapeutic Effect: Inhib- butter) may increase serum phosphate;
its tumor cell growth and metastasis. may affect dose modifications. Restrict
Induces cellular death of tumor cells. phosphate intake to 600–800 mg daily.
E LAB VALUES: May increase serum alka-
PHARMACOKINETICS line phosphatase, ALT, AST, calcium,
Widely distributed. Metabolized in liver. creatinine, glucose, potassium. May
Protein binding: 99.8%. Peak plasma decrease serum albumin, sodium; Hgb,
concentration: 2.5 hrs. Steady state leukocytes, neutrophils, platelets. May
reached in 2 wks. Excreted in feces increase or decrease serum phosphate.
(69%), urine (19%). Half-life: 59 hrs.
AVAILABILITY (Rx)
LIFESPAN CONSIDERATIONS Tablets: 3 mg, 4 mg, 5 mg.
Pregnancy/Lactation: Avoid preg-
nancy; may cause fetal harm. Female ADMINISTRATION/
pts and male pts with female partners HANDLING
of reproductive potential should use PO
effective contraception during treatment • Give without regard to food. Adminis-
and up to 1 mo after discontinuation. ter tablets whole; do not break, cut,
Unknown if distributed in breast milk. crush, or divide. Tablets should not be
Breastfeeding not recommended dur- chewed. • If a dose is missed, give as
ing treatment and for at least 1 mo after soon as possible. If vomiting occurs after
discontinuation. May impair fertility in administration, give next dose at regu-
female pts. Children: Safety and efficacy larly scheduled time.
not established. Elderly: No age-related
precautions noted. INDICATIONS/ROUTES/
DOSAGE
INTERACTIONS Note: Assess serum phosphate levels
DRUG: Strong CYP3A4 inhibitors 14–21 days after therapy initiation.
(e.g., clarithromycin, ketocon- ­Restrict phosphate intake to 600–800
azole), moderate CYP3A inhibitors mg daily
(e.g., ciprofloxacin, dilTIAZem, flu-
conazole, verapamil) may increase Urothelial Carcinoma
concentration/effect. Strong CYP3A4 PO: ADULTS, ELDERLY: Initially, 8 mg once
inducers (e.g., carBAMazepine, phe- daily. After 14–21 days, increase dose to
nytoin, rifAMPin) may decrease con- 9 mg once daily if serum phosphate is
centration/effect. Phosphate-altering less than 5.5 mg/dL and there are no
drugs (e.g., ergocalciferol, K-phos, ocular toxicities or Grade 2 (or higher)
PhosLo, Renagel) may alter phosphate adverse reactions. Continue until disease
level; may affect dose modifications. progression or unacceptable toxicity.

Dose Reduction Schedule for Adverse Reactions


First Dose Second Dose Third Dose Fourth Dose Fifth Dose
Dose Reduction Reduction Reduction Reduction Reduction
9 mg 8 mg 6 mg 5 mg 4 mg Discontinue
8 mg 6 mg 5 mg 4 mg Discontinue N/A

underlined – top prescribed drug


erdafitinib 439
Dose Modification resume at next lower dose level. Any
Based on Common Terminology Criteria Grade 4 reaction: Permanently discon-
for Adverse Events (CTCAE). tinue.
Hyperphosphatemia Dosage in Renal Impairment
Serum phosphate 5.6–6.9 mg/dL Mild to moderate impairment: No
(1.8–2.3 mmol/L): Maintain dose. dose adjustment. Severe impairment:
7–9 mg/dL (2.3–2.9 mmol/L): With- Not specified; use caution. E
hold treatment until serum phosphate
is less than 5.5 mg/dL (or baseline), Dosage in Hepatic Impairment
then resume at same dose. May reduce Mild impairment: No dose adjustment.
dose if hyperphosphatemia lasts greater Moderate to severe impairment: Not
than 1 wk. Greater than 9 mg/dL and specified; use caution.
less than 10 mg/dL (greater than
2.9 mmol/L): Withhold treatment until SIDE EFFECTS
serum phosphate is less than 5.5 mg/ Frequent (56%–20%): Stomatitis, fatigue,
dL (or baseline), then resume at next asthenia, lethargy, malaise, diarrhea,
lower dose level. Greater than 10 mg/ dry mouth, onycholysis, onychocla-
dL (greater than 3.2 mmol/L); sig- sis, nail disorder, nail dystrophy, nail
nificant change of baseline renal ridging, decreased appetite, dysgeusia,
function; Grade 3 hypercalcemia: constipation, dry eye, alopecia, abdom-
Withhold treatment until serum phos- inal pain, nausea, musculoskeletal
phate is less than 5.5 mg/dL (or base- pain, back/chest/neck pain. Occasional
line), then resume at 2 lower dose levels. (17%–10%): Blurry vision, decreased
weight, cachexia, pyrexia, vomiting,
Serious Retinopathy/Retinal Pigment nail discoloration, oropharyngeal pain,
Epithelial Detachment arthralgia, increased lacrimation, dys-
Asymptomatic; clinical of diagnostic pnea.
observation: Withhold treatment until
resolved. Resume at next lower dose level ADVERSE EFFECTS/TOXIC
if resolved within 4 wks. Consider re-esca- REACTIONS
lation of dose if symptoms do not recur for Hemoglobinemia, leukopenia, neutro-
1 mo. If stable but not resolved for 2 con- penia, thrombocytopenia is an ex-
secutive eye exams, resume at next lower pected response to therapy. Ocular
dose level. Visual acuity 20/40 (or bet- toxicities including serious retinopa-
ter) or greater than or equal to 3 lines thy/retinal pigment epithelial detach-
of decreased vision from baseline: ment reported in 25% of pts. Ocular
Withhold treatment until resolved. Resume disorders including keratitis, foreign
at next lower dose level if resolved within body sensation, corneal erosion re-
4 wks. Visual acuity worse than 20/40 ported in 28% of pts. Grade 3 serious
or greater than 3 lines of decreased retinopathy/retinal pigment epithelial
vision from baseline: Withhold treat- detachment reported in 3% of pts. Hy-
ment until resolved. Resume at 2 lower perphosphatemia reported in 76% of
dose levels if resolved within 4 wks. Con- pts with 32% of pts requiring oral
sider permanent discontinuation if recur- phosphate binders. Palmar-plantar
rent. Visual acuity 20/200 or worse in erythrodysesthesia syndrome reported
affected eye: Permanently discontinue. in 26% of pts. Hematuria reported in
11% of pts. Infections including paro-
Other Adverse Reactions nychia (17% of pts), urinary tract in-
Any Grade 3 reaction: Withhold treat- fection (17% of pts), conjunctivitis
ment until improved to grade 1 or 0, than (11% of pts) may occur.

Canadian trade name Non-Crushable Drug High Alert drug


440 erenumab-aooe

NURSING CONSIDERATIONS symptoms of bone marrow depression


such as bruising, fatigue, fever, shortness
BASELINE ASSESSMENT of breath, weight loss; bleeding easily,
Obtain CBC, BMP, LFTs, serum phosphate bloody urine or stool. • Expect frequent
level; pregnancy test in female pts of re- eye exams, skin exams. Immediately re-
productive potential. Confirm presence port vision changes of any kind. • Treat-
of susceptible FGFR genetic alterations ment may cause fetal harm. Female pts
E in tumor specimens. Verify compliance and male pts with female partners of
of effective contraception in female pts childbearing potential should use effective
and male pts with female partners of contraception during treatment and up to
reproductive potential. Obtain visual 1 mo after last dose. Do not breast-
acuity. Screen for active infection. Ques- feed. • Limit intake of phosphorus-con-
tion history of hepatic/renal impairment, taining food unless blood tests verify ac-
optic disorders. Receive full medication ceptable phosphate levels. • Report liver
history and screen for interactions. Offer problems such as bruising, confusion,
emotional support. dark or amber-colored urine, right upper
abdominal pain, or yellowing of the skin
INTERVENTION/EVALUATION
or eyes; symptoms of UTI (burning with
Monitor CBC, BMP, LFTs, serum ionized urination, fever, urinary frequency, foul-
calcium periodically. Obtain serum phos- smelling or cloudy urine). • There is a
phate level 14–21 days after initiation. high risk of interactions with other medi-
Restrict phosphorus intake to 600–800 cations. Do not take any newly prescribed
mg daily. If serum phosphate is greater medications unless approved by pre-
than 7 mg/dL, consider administration scriber who originally started treat-
of an oral phosphate binder until serum ment. • Avoid grapefruit products,
phosphate is less than 5.5 mg/dL. Obtain herbal supplements (esp. St. John’s wort).
weekly serum phosphate levels in pts
who develop hyperphosphatemia. Moni-
tor for symptoms of hyperphosphatemia,
which may mimic symptoms of hypocal- erenumab-aooe
cemia (facial twitching, muscle cramps,
numbness of hand, feet, lips; seizures). e-ren-ue-mab-aooe
Assess skin for dermal toxicities. Monthly (Aimovig)
ophthalmologic exams (including visual Do not confuse erenumab with
acuity, slit lamp examination, fundoscopy, aducanumab or secukinumab.
optical coherence tomography) should
be perform by a specialist for the first uCLASSIFICATION
4 mos, then q3mos thereafter, or emer- PHARMACOTHERAPEUTIC: Calci-
gently if new symptoms occur. Obtain tonin gene-related peptide (CGRP)
urinalysis if UTI is suspected (dysuria, receptor antagonist. Monoclonal an-
fever, foul-smelling or cloudy urine, uri- tibody. CLINICAL: Migraine prophy-
nary frequency). Diligently monitor for laxis agent.
infections.
PATIENT/FAMILY TEACHING USES
• Treatment may depress your immune Preventative treatment of migraines in adults.
system and reduce your ability to fight in-
fection. Report symptoms of infection PRECAUTIONS
such as body aches, burning with urina- Contraindications: Hypersensitivity to
tion, chills, cough, fatigue, fever. Avoid erenumab-aooe. Cautions: Latex allergy
those with active infection. • Report (when handling needle cap).

underlined – top prescribed drug


erenumab-aooe 441

ACTION do not place back into refrigerator. • Do


Binds to and inhibits calcitonin gene- not freeze or expose to heating sources. •
related peptide (CGRP) receptor. Thera- Do not shake. • Protect from light.
peutic Effect: Reduces occurrence of
INDICATIONS/ROUTES/DOSAGE
acute or chronic migraine headaches.
Acute or Chronic Migraine Headaches
PHARMACOKINETICS SQ: ADULTS: 70 mg once monthly. May
Widely distributed. Peak plasma concen- increase to 140 mg once monthly if 70 E
tration: 6 days. Steady state reached by 3 mg dose is ineffective.
mos of dosing. Eliminated mainly via pro- Dosage in Renal Impairment
teolytic degradation. Half-life: 28 days. Mild to moderate impairment: No
LIFESPAN CONSIDERATIONS dose adjustment. Severe impairment:
Not specified; use caution.
Pregnancy/Lactation: Unknown if dis-
tributed in breast milk. Children: Safety Dosage in Hepatic Impairment
and efficacy not established. Elderly: Not specified; use caution.
Not specified.
SIDE EFFECTS
INTERACTIONS Occasional (6%–1%): Injection site pain/
DRUG: May enhance the adverse/toxic erythema, constipation, cramps, muscle
effect of belimumab. HERBAL: None spasm.
significant. FOOD: None known. LAB
VALUES: None known. ADVERSE EFFECTS/TOXIC
REACTIONS
AVAILABILITY (Rx) Immunogenicity (auto-erenumab anti-
Injection Solution: 70 mg/1 mL in pre- bodies) occurred in 6.2% of pts.
filled syringe or autoinjector.
NURSING CONSIDERATIONS
ADMINISTRATION/HANDLING
BASELINE ASSESSMENT
SQ
Preparation • Remove prefilled syringe Question characteristics of migraine
or autoinjector from refrigerator and headaches (onset, location, duration,
allow solution to warm to room tempera- possible precipitating symptoms). Ques-
ture (approx. 30 mins) with needle cap tion history of latex allergy. Assess pt’s
intact. • Visually inspect for particulate willingness to self-inject medication.
matter or discoloration. Solution should INTERVENTION/EVALUATION
appear clear, colorless to slightly yellow in Evaluate for relief of migraine headache
color. Do not use if solution is cloudy, dis- and resulting photophobia, phonophobia
colored, or visible particles are observed. (sound sensitivity), nausea, vomiting,
Administration • Insert needle subcu- dizziness, fogginess.
taneously into upper arm, outer thigh, or
abdomen and inject solution. • Do not PATIENT/FAMILY TEACHING
inject into areas of active skin disease • Latex needle cap may cause a skin re-
or injury such as sunburns, skin rashes, action in pts with a latex allergy if direct
inflammation, skin infections, or active skin contact is made. • A healthcare
psoriasis. • Do not administer IV or provider will show you how to properly
intramuscularly. • Rotate injection sites. prepare and inject medication. You must
Storage • Refrigerate prefilled syringes demonstrate correct preparation and in-
in original carton until time of use. • May jection techniques before using medica-
store at room temperature for up to 7 tion at home.
days. Once warmed to room temperature,
Canadian trade name Non-Crushable Drug High Alert drug
442 eriBULin

INTERACTIONS
eriBULin DRUG: May decrease levels/effects of
BCG (intravesical). QT-prolonging
er-i-bue-lin
medications (e.g., amiodarone,
(Halaven)
ciprofloxacin, haloperidol, keto-
Do not confuse eriBULin with
conazole) may increase risk of QT
epiRUBicin or erlotinib.
prolongation. HERBAL: None significant.
E FOOD: None known. LAB VALUES: May
uCLASSIFICATION
decrease WBC, Hgb, Hct, platelet count,
PHARMACOTHERAPEUTIC: Microtu-
potassium. May increase ALT.
bule inhibitor. CLINICAL: Antineo-
plastic. AVAILABILITY (Rx)
Injection, Solution: 1 mg/2 mL (0.5 mg/
USES mL).
Treatment of metastatic breast cancer in ADMINISTRATION/HANDLING
pts who previously received at least 2 che-
motherapeutic regimens for treatment. IV
Treatment of metastatic liposarcoma in Reconstitution • May administer un-
pts who received a prior anthracycline- diluted or dilute in 100 mL 0.9% NaCl.
containing regimen. Rate of administration • Administer
over 2–5 min.
PRECAUTIONS Storage • Store at room tempera-
Contraindications: Hypersensitivity to ture. • Once diluted, syringe or diluted
eriBULin. Cautions: Prolonged QTc (con- solution may be stored for up to 4 hrs at
genital, other medications that prolong QT room temperature or up to 24 hrs if re-
interval), hypokalemia, hypomagnesemia, frigerated.
hepatic/renal impairment, moderate to
severe neuropathy, HF. IV INCOMPATIBILITIES
Do not dilute with D5W or administer
ACTION through IV line containing solutions with
Inhibits growth phase of microtubule by dextrose or in same IV line with other
inhibiting formation of mitotic spindles. medications.
Causes mitotic blockage and arrests the
cell cycle. Therapeutic Effect: Blocks INDICATIONS/ROUTES/DOSAGE
cells in mitotic phase of cell division, Metastatic Breast Cancer, Liposarcoma
leading to cell death. IV: ADULTS, ELDERLY: 1.4 mg/m2 over
2–5 min on days 1 and 8 of 21-day cycle.
PHARMACOKINETICS
Extensively metabolized in liver. Protein Dosage in Renal Impairment
binding: 49%–65%. Excreted in feces Mild impairment: No dose adjust-
(82%), urine (9%). Half-life: 40 hrs. ment. Moderate to severe impair-
ment: CrCl 15–49 mL/min: 1.1 mg/
LIFESPAN CONSIDERATIONS m2/dose.
Pregnancy/Lactation: May cause
embryo-fetal toxicity. Unknown if dis- Dosage in Hepatic Impairment
tributed in breast milk. Children: Safety Mild impairment: 1.1 mg/m2/dose.
and efficacy not established in pts Moderate im­­pairment: 0.7 mg/m2/
younger than 18 yrs. Elderly: No age- dose. Severe im­­pairment: Use not
related precautions noted. recommended.

underlined – top prescribed drug


erlotinib 443
Recommended Dose Delays sensation, hyperesthesia, hypoesthesia,
Do not administer day 1 or day 8 of treat- paresthesia, discomfort, neuropathic
ment for any of the following: ANC less pain). Assess hands, feet for erythema.
than 1,000 cells/mm3, platelets less than Monitor CBC for evidence of neutropenia,
75,000 cells/mm3, Grade 3 or 4 nonhe- thrombocytopenia. Assess mouth for sto-
matologic toxicities. Day 8 dose may be matitis (erythema, ulceration, mucosal
delayed for maximum of 1 wk. If toxici- burning).
ties do not resolve or improve to Grade 2 E
severity by day 15, omit dose. If toxicities PATIENT/FAMILY TEACHING
resolve or improve to Grade 2 severity by • Avoid crowds, those with known infec-
day 15, continue treatment at reduced tion. • Avoid contact with anyone who
dose and initiate next cycle no sooner recently received live virus vac-
than 2 wks later. Do not re-escalate dose cine. • Do not have immunizations
after it has been reduced. without physician’s approval (drug low-
ers body resistance). • Promptly report
SIDE EFFECTS fever over 100.5°F, chills, cough, burning
Common (54%–35%): Fatigue, asthenia, or pain urinating, numbness, tingling,
alopecia, peripheral sensory neuropathy, burning sensation, erythema of hands/
nausea. Frequent (25%–18%): Constipa- feet. • Women of reproductive poten-
tion, arthralgia/myalgia, decreased weight, tial should use effective contraception
anorexia, pyrexia, headache, diarrhea, during and for 2 wks following last dose
vomiting. Occasional (16%–9%): Back of eribulin; males with female partners of
pain, dyspnea, cough, bone pain, extrem- reproductive potential should use effec-
ity pain, urinary tract infection, oral muco- tive contraception during and for 3.5
sal inflammation. mos following last dose of eribulin.
ADVERSE EFFECTS/TOXIC
REACTIONS
Neutropenia occurs in 82% of pts, with erlotinib
57% developing Grade 3 neutropenia.
Severe neutropenia (ANC less than 500 er-loe-ti-nib
cells/mm3) lasting more than 1 wk (Tarceva)
occurred in 12%. Anemia occurs in 58% Do not confuse erlotinib with
of pts. Peripheral neuropathy occurs dasatinib, eriBULin, gefitinib,
in 8% of pts but is the most common imatinib, or lapatinib.
adverse reaction requiring discontinu-
ation of therapy. Prolonged QTc may be uCLASSIFICATION
noted on or after day 8 of treatment. PHARMACOTHERAPEUTIC: Epider-
mal growth factor receptor (EGFR)
NURSING CONSIDERATIONS inhibitor; tyrosine kinase inhibitor.
CLINICAL: Antineoplastic.
BASELINE ASSESSMENT
Question for possibility of pregnancy. Ob-
tain baseline CBC, serum chemistries be- USES
fore treatment begins. Obtain CBC prior Treatment of locally advanced or metastatic
to each dose. Offer emotional support. non–small-cell lung cancer (NSCLC) after
INTERVENTION/EVALUATION failure of at least one prior chemotherapy
regimen (as monotherapy). First-line
Diligently monitor for neutropenia, pe-
treatment of locally advanced, unresect-
ripheral neuropathy (most frequent
able, or metastatic pancreatic cancer (in
cause of drug discontinuation). Monitor
combination with gemcitabine).
for symptoms of neuropathy (burning
Canadian trade name Non-Crushable Drug High Alert drug
444 erlotinib

PRECAUTIONS AVAILABILITY (Rx)


Contraindications: Hypersensitivity to Tablets: 25 mg, 100 mg, 150 mg.
erlotinib. Cautions: Severe hepatic/renal
impairment, cardiovascular disease. ADMINISTRATION/HANDLING
Concurrent use of strong CYP3A4 inhibi- PO
tors and inducers or CYP1A2 inhibitors, • Give at least 1 hr before or 2 hrs after
pts at risk for GI perforation (e.g., peptic ingestion of food. • Avoid grapefruit
E ulcer disease, diverticular disease). Total products. • May dissolve in 3–4 oz water
serum bilirubin greater than 3 times and give orally or via feeding tube. • Give
upper limit of normal. 10 hrs after or 2 hrs before H2 antagonists
(e.g., raNITIdine), proton pump inhibitors
ACTION (e.g., omeprazole, pantoprazole).
Reversibly inhibits overall epidermal
growth factor receptor (EGFR)–tyrosine INDICATIONS/ROUTES/DOSAGE
kinase activity. Inhibits intracellular phos- b ALERT c Dosage adjustment for tox-
phorylation. Therapeutic Effect: Pro- icity: Reduce dose in 50-mg increments.
duces tumor cell death.
NSCLC
PHARMACOKINETICS PO: ADULTS, ELDERLY: 150 mg/day until
About 60% is absorbed after PO admin- disease progression or unacceptable tox-
istration; bioavailability is increased by icity occurs.
food to almost 100%. Metabolized in
Pancreatic Cancer
liver. Protein binding: 93%. Excreted
in feces (83%), urine (8%). Half- PO: ADULTS, ELDERLY: 100 mg/day, in
life: 24–36 hrs. combination with gemcitabine, until dis-
ease progression or unacceptable toxicity
LIFESPAN CONSIDERATIONS occurs.
Pregnancy/Lactation: Unknown if Dosage in Renal Impairment
drug crosses placenta or is distributed Interrupt dosing for Grade 3 or 4 renal
in breast milk. Children: Safety and effi- toxicity during treatment.
cacy not established. Elderly: No age-
related precautions noted. Dosage in Hepatic Impairment
Use extreme caution. Reduce starting
INTERACTIONS dose to 75 mg and individualize dose
DRUG: Strong CYP3A4 inhibitors escalation if tolerated.
(e.g., clarithromycin, ketoconazole,
ritonavir) may increase concentra- SIDE EFFECTS
tion/effects. Strong CYP3A4 inducers Frequent (greater than 10%): Fatigue, anxi-
(e.g., carBAMazepine, phenytoin, ety, headache, depression, insomnia, rash,
rifAMPin) may decrease concentra- pruritus, dry skin, erythema, diarrhea,
tion/effect. Antacids, proton pump anorexia, nausea, vomiting, mucositis, con-
inhibitors (e.g., omeprazole, pan- stipation, dyspepsia, weight loss, dyspha-
toprazole), H2 antagonists (e.g., gia, abdominal pain, arthralgia, dyspnea,
raNITIdine) may decrease absorp- cough. Occasional (10%–1%): Keratitis.
tion/effect. HERBAL: St. John’s wort Rare (less than 1%): Corneal ulceration.
may decrease concentration/effect.
FOOD: Grapefruit products may ADVERSE EFFECTS/TOXIC
increase potential for myelotoxicity. LAB REACTIONS
VALUES: May increase serum bilirubin, UTI occurs occasionally. Pneumonitis, GI
ALT, AST. bleeding occur rarely.

underlined – top prescribed drug


ertapenem 445

NURSING CONSIDERATIONS clostridioforme, Peptostreptococcus


spp., including moderate to severe intra-
BASELINE ASSESSMENT abdominal, skin/skin structure infec-
Obtain CBC, BMP, LFT; pregnancy test in tions; community-acquired pneumonia;
females of reproductive potential. Ques- complicated UTI; acute pelvic infection;
tion history of hepatic/renal impairment, adult diabetic foot infections without
peptic ulcer disease, diverticulosis. Re- osteomyelitis. Prevention of surgical site
ceive full medication history and screen infection. OFF-LABEL: Treatment of IV E
for interactions. Offer emotional support. catheter–related bloodstream infection;
prosthetic joint infection.
INTERVENTION/EVALUATION
Obtain CBC, BMP, LFT periodically. Moni- PRECAUTIONS
tor hydration status. Encourage fluid in- Contraindications: Hypersensitivity
take. Monitor weight, I&Os. to ertapenem. History of anaphylactic
PATIENT/FAMILY TEACHING
hypersensitivity to beta-lactams (e.g.,
imipenem, meropenem), hypersensi-
• Take drug on empty stomach. • Take tivity to amide-type local anesthetics
10 hrs after or 2 hrs before antacid medi- (e.g., lidocaine) (IM use only). Cau-
cations. • Report rash, blood in stool, tions: Hypersensitivity to penicillins,
diarrhea, irritated eyes, fever. • Avoid cephalosporins, renal impairment, CNS
grapefruit products. • Do not breast- disorders (brain lesions or history of sei-
feed. • Use effective contraception dur- zure disorder), elderly.
ing therapy and for at least 1 mo after final
dose. • Report symptoms of UTI, kidney ACTION
infection (e.g., burning while urinating, Penetrates bacterial cell wall of micro-
cloudy or foul-smelling urine, pelvic pain, organisms, binds to penicillin-binding
back pain). proteins, inhibiting cell wall synthesis.
Therapeutic Effect: Produces bacte-
rial cell death.
ertapenem PHARMACOKINETICS
Almost completely absorbed after IM
er-ta-pen-em administration. Protein binding: 85%–
(INVanz) 95%. Widely distributed. Primarily excreted
Do not confuse ertapenem with in urine (80%), feces (10%). Removed by
doripenem, imipenem, or mero- hemodialysis. Half-life: 4 hrs.
penem, or INVanz with AVINza.
LIFESPAN CONSIDERATIONS
uCLASSIFICATION
Pregnancy/Lactation: Distributed in
PHARMACOTHERAPEUTIC: Carbap- breast milk. Children: Safety and effi-
enem. CLINICAL: Antibiotic. cacy not established in pts younger than
18 yrs. Elderly: Advanced or end-stage
USES renal insufficiency may require dosage
adjustment.
Treatment of susceptible infections due to
S. aureus (methicillin-susceptible only), INTERACTIONS
S. agalactiae, S. pneumoniae (peni- DRUG: Probenecid may increase con-
cillin-susceptible only), S. pyogenes, centration/effect. May decrease concen-
E. coli, H. influenzae (beta-lactamase tration/effect of valproic acid, BCG
negative strains only), K. pneumoniae, (intravesical). HERBAL: None significant.
M. catarrhalis, Bacteroides spp., C. FOOD: None known. LAB VALUES: May

Canadian trade name Non-Crushable Drug High Alert drug


446 ertapenem
increase serum alkaline phosphatase, ALT, Dosage in Renal Impairment
AST, bilirubin, BUN, creatinine, glucose, CrCl 30 mL/min 500 mg once daily
PT, aPTT, sodium. May decrease platelet or less
count, Hgb, Hct, WBC. Hemodialysis If daily dose given within
6h prior to HD, give 150
AVAILABILITY (Rx) mg dose after HD.
Injection, Powder for Reconstitution: 1 g. Peritoneal 500 mg once daily
E ­dialysis
ADMINISTRATION/HANDLING
IV Dosage in Hepatic Impairment
No dose adjustment.
Reconstitution • Dilute 1-g vial with
10 mL 0.9% NaCl or Bacteriostatic Water SIDE EFFECTS
for Injection. • Shake well to dis- Frequent (10%–6%): Diarrhea, nausea,
solve. • Further dilute with 50 mL 0.9% headache. Occasional (5%–2%): Altered
NaCl (maximum concentration: 20 mental status, insomnia, rash, abdominal
mg/mL). pain, constipation, chest pain, vomiting,
Rate of administration • Give by in- edema, fever. Rare (less than 2%): Diz-
termittent IV infusion (piggyback). Do ziness, cough, oral candidiasis, anxiety,
not give IV push. • Infuse over 30 min. tachycardia, phlebitis at IV site.
Storage • Solution appears colorless
to yellow (variation in color does not af- ADVERSE EFFECTS/TOXIC
fect potency). • Discard if solution REACTIONS
contains precipitate. • Reconstituted Antibiotic-associated colitis, other superin-
solution is stable for 6 hrs at room tem- fections (abdominal cramps, severe watery
perature or 24 hrs if refrigerated. diarrhea, fever) may result from altered
bacterial balance in GI tract. Anaphylactic
IM reactions have been reported. Seizures
• Reconstitute with 3.2 mL 1% lidocaine may occur in pts with CNS disorders (brain
HCl injection (without EPINEPH- lesions, history of seizures), bacterial men-
rine). • Shake vial thoroughly. • In- ingitis, severe renal impairment.
ject deep in large muscle mass (gluteal
or lateral part of thigh). • Administer NURSING CONSIDERATIONS
suspension within 1 hr after preparation.
BASELINE ASSESSMENT
IV INCOMPATIBILITIES Question for history of allergies, particu-
Do not mix or infuse with any other medi- larly to beta-lactams, penicillins, cephalo-
cations. Do not use diluents or IV solu- sporins. Inquire about history of seizures.
tions containing dextrose. INTERVENTION/EVALUATION
IV COMPATIBILITIES Monitor WBC count. Monitor renal/hepatic
Heparin, potassium chloride, tigecycline function. Monitor daily pattern of bowel ac-
(Tygacil), Sterile Water for Injection, tivity, stool consistency. Monitor for nausea,
0.9% NaCl. vomiting. Evaluate hydration status. Evaluate
for inflammation at IV injection site. Assess
INDICATIONS/ROUTES/DOSAGE skin for rash. Observe mental status; be alert
Usual Dosage Range to tremors, possible seizures. Assess sleep
IM, IV: ADULTS, ELDERLY, CHILDREN 13 YRS pattern for evidence of insomnia.
AND OLDER: 1 g/day. CHILDREN 3 MOS–12 PATIENT/FAMILY TEACHING
YRS: 15 mg/kg 2 times/day. Maxi-
• Report tremors, seizures, rash, prolonged
mum: 500 mg/dose. diarrhea, chest pain, other new symptoms.
underlined – top prescribed drug
ertugliflozin 447

PHARMACOKINETICS
ertugliflozin Readily absorbed. Metabolized in liver
by glucuronidation. Protein binding:
er-too-gli-floe-zin
94%. Peak plasma concentration: 1 hr.
(Steglatro)
Excreted in urine (50%), feces (41%).
Do not confuse ertugliflozin
Half-life: 17 hrs.
with canagliflozin, dapagliflo-
zin, or empagliflozin. LIFESPAN CONSIDERATIONS E
FIXED-COMBINATIONS Pregnancy/Lactation: Not recom-
mended in second or third trimester.
Segluromet: ertugliflozin/metformin
Unknown if distributed in breast milk.
(an antidiabetic): 2.5 mg/500 mg.
Breastfeeding not recommended. Chil-
Steglujan: ertugliflozin/sitagliptin (an
dren: Safety and efficacy not estab-
antidiabetic): 5 mg/100 mg.
lished. Elderly: May have increased
uCLASSIFICATION risk for adverse reactions (dehydration,
hypotension, syncope).
PHARMACOTHERAPEUTIC: Sodium-
glucose co-transporter 2 (SGLT2) INTERACTIONS
inhibitor. CLINICAL: Antidiabetic.
DRUG: Insulin, insulin secretagogues
(e.g., glyBURIDE) may increase risk of
USES hypoglycemia. HERBAL: None significant.
FOOD: None known. LAB VALUES: May
Adjunctive treatment to diet and exercise
to improve glycemic control in pts with increase low-density lipoprotein cho-
type 2 diabetes mellitus. lesterol (LDL-C), serum creatinine. May
decrease eGFR.
PRECAUTIONS
AVAILABILITY (Rx)
Contraindications: Hypersensitivity to
ertugliflozin, other SGLT2 inhibitors; Tablets: 5 mg, 15 mg.
severe renal impairment (eGFR less ADMINISTRATION/HANDLING
than 30 mL/min), ESRD, dialysis. Cau-
PO
tions: Concurrent use of diuretics, other
hypoglycemic medications; mild to mod- • Give without regard to food in the
erate renal impairment (CrCl less than 30 morning.
mL/min), hypovolemia (anemia, dehy- INDICATIONS/ROUTES/DOSAGE
dration), elderly; pts with low systolic
Type 2 Diabetes Mellitus
B/P, hyperlipidemia. Pts at risk for lower
PO: ADULTS, ELDERLY: Initially,
5 mg once
leg amputation (diabetic foot ulcers,
peripheral vascular disease, neuropathy). daily in the morning. May increase dose
History of genital mycotic infection. Not based on tolerability. Maximum: 15 mg/
recommended in pts with diabetic keto- day.
acidosis, type 1 diabetes mellitus. Dosage in Renal Impairment
eGFR greater than 60 mL/min: No
ACTION dose adjustment. eGFR 30–59 mL/min:
Inhibits SGLT2 in proximal renal Not recommended. eGFR less than 30
tubule, reducing reabsorption of fil- mL/min: Contraindicated.
tered glucose from tubular lumen
and lowering renal threshold for glu- Dosage in Hepatic Impairment
cose. Therapeutic Effect: Increases Mild to moderate impairment: No
urinary excretion of glucose, lowers dose adjustment. Severe impairment:
serum glucose levels. Not specified; use caution.

Canadian trade name Non-Crushable Drug High Alert drug


448 erythromycin

SIDE EFFECTS (anxiety, confusion, diaphoresis, diplo-


Rare (2%–less than 1%): Headache, pia, dizziness, headache, hunger, perioral
increased urination, nasopharyngitis, numbness, tachycardia, tremors); hyper-
back pain, decreased weight, thirst, dry glycemia (fatigue, Kussmaul respirations,
mouth, polydipsia, dry throat. polyphagia, polyuria, polydipsia, nausea,
vomiting). Concomitant use of beta block-
ADVERSE EFFECTS/TOXIC ers (e.g., carvedilol, metoprolol) may
E REACTIONS mask symptoms of hypoglycemia. Moni-
Symptomatic hypotension (orthostatic tor for acute kidney injury (dark-colored
hypotension, postural dizziness, syn- urine, flank pain, decreased urine output,
cope) may occur, esp. in pts who are muscle aches). Screen for glucose-alter-
elderly, use diuretics, or have low sys- ing conditions: fever, increased activity
tolic B/P. Fatal cases of ketoacidosis have or stress, surgical procedures. Obtain
occurred. Intravascular volume deple- dietary consult for nutritional education.
tion/contraction may cause acute kidney Encourage fluid intake. Monitor weight,
injury requiring dialysis. Hypoglycemic I&Os.
events were reported, esp. in pts using PATIENT/FAMILY TEACHING
concomitant hypoglycemic medications
• Diabetes mellitus requires lifelong con-
that cause hypoglycemia. Infections
trol. Diet and exercise are principal parts
including urosepsis, pyelonephritis, UTI,
of treatment; do not skip or delay meals.
genital mycotic infections (male and
• Test blood sugar regularly. • Monitor
female), upper respiratory tract infection
daily calorie intake. • When taking com-
may occur. May increase risk of lower
bination drug therapy or when glucose
limb amputations.
demands are altered (fever, infection,
NURSING CONSIDERATIONS trauma, stress), have low blood sugar
treatment readily available (glucagon,
BASELINE ASSESSMENT oral dextrose). • Go slowly from lying
Obtain BUN, serum creatinine, eGFR, to standing to prevent dizziness. • Gen-
CrCl; capillary blood glucose, Hgb A1c; ital itching may indicate yeast infec-
B/P. Correct volume-depletion before tion. • Therapy may increase risk for
initiation. Assess pt’s understanding of dehydration/low blood pressure, which
diabetes management, routine home may cause kidney failure. Immediately
glucose monitoring. Receive full medica- report decreased urination, amber-col-
tion history and screen for interactions. ored urine, flank pain, fatigue, swelling
Question plans of breastfeeding. Ques- of the hands or feet. • Report symp-
tion history of renal impairment. Screen toms of UTI, kidney infection (e.g., burn-
for risks of lower limb amputation (e.g., ing while urinating, cloudy or foul-smell-
peripheral vascular disease, diabetic foot ing urine, pelvic pain, back pain). • Do
ulcers, neuropathy). not breastfeed.
INTERVENTION/EVALUATION
Obtain BUN, serum creatinine, eGFR,
CrCl; capillary blood glucose, Hgb A1c erythromycin
periodically. Monitor for symptoms of ke-
toacidosis (e.g., dehydration, confusion, er-ith-roe-mye-sin
extreme thirst, fruity breath, Kussmaul (Akne-Mycin, Apo-Erythro Base ,
respirations, nausea). Pts presenting with EES, Erybid , Eryc, EryDerm,
metabolic acidosis should be screened EryPed, Ery-Tab, Erythrocin, PCE
for ketoacidosis, regardless of serum Dispertab)
glucose levels. Assess for hypoglycemia

underlined – top prescribed drug


erythromycin 449
Do not confuse Eryc with Emcyt, inhibiting RNA-dependent protein synthe-
or erythromycin with azithro- sis. Therapeutic Effect: Bacteriostatic.
mycin or clarithromycin.
PHARMACOKINETICS
FIXED-COMBINATION(S) Variably absorbed from GI tract (depend-
Eryzole, Pediazole: erythromycin/ ing on dosage form used). Protein bind-
sulfiSOXAZOLE (sulfonamide): 200 ing: 70%–90%. Widely distributed.
mg/600 mg per 5 mL. Metabolized in liver. Primarily eliminated E
in feces by bile. Not removed by hemodi-
uCLASSIFICATION alysis. Half-life: 1.4–2 hrs (increased
PHARMACOTHERAPEUTIC: Mac- in renal impairment).
rolide. CLINICAL: Antibiotic, anti-
acne. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses pla-
centa. Distributed in breast milk. Eryth-
USES romycin estolate may increase hepatic
Treatment of susceptible infections due to enzymes in pregnant women. Children/
S. pyogenes, S. pneumoniae, S. aureus, Elderly: No age-related precautions
M. pneumoniae, Legionella, Chla- noted. High dosage in pts with decreased
mydia, N. gonorrhoeae, E. histolytica, hepatic/renal function increases risk of
including syphilis, nongonococcal ure- hearing loss.
thritis, diphtheria, pertussis, chancroid,
Campylobacter gastroenteritis. Topical: INTERACTIONS
Treatment of acne vulgaris. Ophthalmic: DRUG: May increase concentration/
Prevention of gonococcal ophthalmia effect of bosutinib, budesonide,
neonatorum, superficial ocular infec- busPIRone, cycloSPORINE, calcium
tions. OFF-LABEL: Systemic: Treatment channel blockers (e.g., dilTIAZem,
of acne vulgaris, chancroid, Campy- verapamil), statins (e.g., atorvas-
lobacter enteritis, gastroparesis, Lyme tatin, simvastatin). Amiodarone,
disease, preoperative gut sterilization. dronedarone, fluconazole may
Topical: Treatment of minor bacterial increase QT interval–prolonging effect.
skin infections. Ophthalmic: Treatment Strong CYP3A4 inducers (e.g., car-
of blepharitis, conjunctivitis, keratitis, BAMazepine, phenytoin, rifAMPin)
chlamydial trachoma. may decrease concentration/effect.
HERBAL: St. John’s wort may decrease
PRECAUTIONS concentration. FOOD: None known. LAB
Contraindications: Hypersensitivity to VALUES: May increase serum alkaline
eryth­­romycin. Concomitant administra- phosphatase, bilirubin, ALT, AST.
tion with ergot derivatives, lovastatin,
pimozide, simvastatin. Cautions: Elderly, AVAILABILITY (Rx)
myasthenia gravis, strong CYP3A4 Gel, Topical: 2%. Injection, Powder for
inhibitor, hepatic impairment, pts with Reconstitution: 500 mg, 1 g. Ointment,
prolonged QT intervals, uncorrected Ophthalmic: 0.5%. Ointment, Topical:
hypokalemia or hypomagnesemia, con- (Akne-Mycin): 2%. Oral Suspension: (EES,
current use of class IA or III antiarrhyth- EryPed): 200 mg/5 mL, 400 mg/5 mL. Tab-
mics. let as Base: 250 mg, 333 mg, 500 mg.
Tablet as Ethylsuccinate: (EES): 400 mg.
ACTION
Penetrates bacterial cell membranes, Capsules, Delayed-Release (Eryc):
reversibly binds to bacterial ribosomes, 250 mg. Tablets, Delayed-Release (Ery-Tab):
250 mg, 333 mg, 500 mg.

Canadian trade name Non-Crushable Drug High Alert drug


450 erythromycin

ADMINISTRATION/HANDLING INDICATIONS/ROUTES/DOSAGE
IV Usual Dosage Range
PO: ADULTS, ELDERLY: (Base): 250–500
Reconstitution • Reconstitute each mg q6–12h. Maximum: 4 g/day. CHIL-
500 mg with 10 mL Sterile Water for In- DREN: 30–50 mg/kg/day in 2–4 divided
jection without preservative to provide a doses. Maximum: 2 g/day. (Ethylsuc-
concentration of 50 mg/mL. • Further cinate): ADULTS, ELDERLY: 400–800 mg
E dilute with 100–250 mL D5W or 0.9% q6–12h. Maximum: 4 g/day. CHIL-
NaCl to maximum concentration of 5 DREN: 30–50 mg/kg/day in divided
mg/mL. doses. Maximum: 4 g/day. NEO-
Rate of administration • For inter- NATES: 10 mg/kg/dose q8–12h.
mittent IV infusion (piggyback), infuse IV: ADULTS, ELDERLY: 15–20 mg/kg/
over 20–60 min. day divided q6h. Maximum: 4 g/day.
Storage • Store parenteral form at CHILDREN, INFANTS: 15–20 mg/kg/day
room temperature. • Initial reconsti- divided q6h. Maximum: 4 g/day. NEO-
tuted solution in vial is stable for 2 wks NATES: 10 mg/kg/dose q8–12h.
refrigerated or 24 hrs at room tempera-
ture. • Diluted IV solution stable for 8 Dosage in Renal/Hepatic Impairment
hrs at room temperature or 24 hrs if re- No dose adjustment.
frigerated. • Discard if precipitate
forms. SIDE EFFECTS
Frequent: IV: Abdominal cramping/
PO discomfort, phlebitis/thrombophlebi-
• May give with food to decrease GI tis. Topical: Dry skin (50%). Occa-
upset. Do not give with milk or acidic sional: Nausea, vomiting, diarrhea, rash,
beverages. • Oral suspension is stable urticaria. Rare: Ophthalmic: Sensitivity
for 35 days at room temperature. • Do reaction with increased irritation, burning,
not crush delayed-release capsules, itching, inflammation. Topical: Urticaria.
tablets.
ADVERSE EFFECTS/TOXIC
Ophthalmic REACTIONS
• Place gloved finger on lower eyelid Antibiotic-associated colitis, other super-
and pull out until a pocket is formed be- infections (abdominal cramps, severe
tween eye and lower lid. • Place 14–12 watery diarrhea, fever), reversible cho-
inch of ointment into pocket. • Instruct lestatic hepatitis may occur. High dosage
pt to close eye gently for 1–2 min (so that in pts with renal impairment may lead
medication will not be squeezed out of to reversible hearing loss. Anaphylaxis
the sac) and to roll eyeball to increase occurs rarely. Ventricular arrhythmias,
contact area of drug to eye. prolonged QT interval occur rarely with
IV INCOMPATIBILITIES IV form.
Fluconazole (Diflucan), furosemide (Lasix), NURSING CONSIDERATIONS
heparin, metoclopramide (Reglan).
BASELINE ASSESSMENT
IV COMPATIBILITIES Question for history of allergies (particularly
Amiodarone (Cordarone), dilTIAZem erythromycins), hepatitis. Receive full medi-
(Cardizem), HYDROmorphone (Dilau- cation history and screen for interactions.
did), lidocaine, LORazepam (Ativan), INTERVENTION/EVALUATION
magnesium sulfate, midazolam (Versed),
morphine, multivitamins, potassium Monitor daily pattern of bowel activity, stool
chloride. consistency. Assess skin for rash. Assess for

underlined – top prescribed drug


escitalopram 451
hepatotoxicity (malaise, fever, abdominal PRECAUTIONS
pain, GI disturbances). Be alert for super- Contraindications: Hypersensitivity to
infection: fever, vomiting, diarrhea, anal/ escitalopram. Use of MAOI intended
genital pruritus, oral mucosal changes (ul- to treat psychiatric disorders (concur-
ceration, pain, erythema). Check for phle- rent or within 14 days of discontinuing
bitis (heat, pain, red streaking over vein). either escitalopram or MAOI). Initiation
Monitor for high-dose hearing loss. in pts receiving linezolid or IV methylene
blue. Concurrent use with pimozide. E
PATIENT/FAMILY TEACHING
Cautions: Hepatic/renal impairment,
• Continue therapy for full length of treat-
history of seizure disorder, concurrent
ment. • Doses should be evenly
use of CNS depressants, pts at high risk
spaced. • Take medication with 8 oz
of suicide, concomitant aspirin, NSAIDs,
water 1 hr before or 2 hrs following food
warfarin (may potentiate bleeding risk),
or beverage. • Ophthalmic: Report
elderly, metabolic disease; recent history
burning, itching, inflammation. • Topi-
of MI, cardiovascular disease.
cal: Report excessive skin dryness, itch-
ing, burning. • Improvement of acne ACTION
may not occur for 1–2 mos; maximum
Blocks uptake of neurotransmitter sero-
benefit may take 3 mos; therapy may last
tonin at neuronal presynaptic mem-
mos or yrs. • Use caution if using other
branes, increasing its availability at
topical acne preparations containing peel-
postsynaptic receptor sites. Therapeutic
ing or abrasive agents, medicated or abra-
Effect: Antidepressant effect.
sive soaps, cosmetics containing alcohol
(e.g., astringents, aftershave lotion). PHARMACOKINETICS
Well absorbed after PO administration.
Protein binding: 56%. Primarily metabo-
escitalopram lized in liver. Primarily excreted in feces,
with a lesser amount eliminated in urine.
es-sye-tal-o-pram Half-life: 35 hrs.
(Cipralex , Lexapro)
j BLACK BOX ALERT jIncreased LIFESPAN CONSIDERATIONS
risk of suicidal ideation and behavior Pregnancy/Lactation: Distributed
in children, adolescents, young adults in breast milk. Children: May cause
18–24 yrs with major depressive
disorder, other psychiatric disorders. increased anticholinergic effects or hyper-
excitability. Elderly: More sensitive to anti-
uCLASSIFICATION cholinergic effects (e.g., dry mouth), more
PHARMACOTHERAPEUTIC: Selective likely to experience dizziness, sedation,
serotonin reuptake inhibitor. CLINI- confusion, hypotension, hyperexcitability.
CAL: Antidepressant.
INTERACTIONS
DRUG: Alcohol, other CNS depres-
USES sants (e.g., LORazepam, morphine,
Treatment of major depressive disorder. zolpidem) may increase CNS depression.
Treatment of generalized anxiety disorder Linezolid, aspirin, NSAIDs (e.g., ibu-
(GAD). OFF-LABEL: Seasonal affective dis- profen, ketorolac, naproxen), warfa-
order (SAD) in children and adolescents, rin may increase risk of bleeding. MAOIs
pervasive developmental disorders (e.g., may cause serotonin syndrome (autonomic
autism), vasomotor symptoms associated hyperactivity, diaphoresis, excitement,
with menopause. hyperthermia, rigidity, neuroleptic malig-
nant syndrome, coma). SUMAtriptan

Canadian trade name Non-Crushable Drug High Alert drug


452 esmolol
may cause weakness, hyperreflexia, menstrual disorder, abdominal pain, agi-
poor coordination. Strong CYP3A4 tation, decreased libido.
inducers (e.g., carBAMazepine,
phenytoin, rifAMPin) may decrease ADVERSE EFFECTS/TOXIC
concentration/effect. HERBAL: St. John’s REACTIONS
wort may decrease concentration/effect. Overdose manifested as dizziness, drows-
FOOD: None known. LAB VALUES: May iness, tachycardia, confusion, seizures.
E decrease serum sodium.
NURSING CONSIDERATIONS
AVAILABILITY (Rx)
BASELINE ASSESSMENT
Oral Solution: 5 mg/5 mL.
For pts on long-term therapy, LFT, renal
Tablets: 5 mg, 10 mg, 20 mg. function tests, blood counts should be
ADMINISTRATION/HANDLING performed periodically. Observe, record
behavior. Assess psychological status,
PO thought content, sleep pattern, appear-
• Give without regard to food. • Do not ance, interest in environment.
break, crush, dissolve, or divide tablets.
INTERVENTION/EVALUATION
INDICATIONS/ROUTES/DOSAGE Supervise suicidal-risk pt closely dur-
Depression ing early therapy (as depression less-
PO: ADULTS: Initially, 10 mg once ens, energy level improves, suicide
daily in the morning or evening. May potential increases). Assess appear-
increase to 20 mg after a minimum of ance, behavior, speech pattern, level
1 wk. ELDERLY: 10 mg/day. CHILDREN of interest, mood. Monitor for suicidal
12–17 YRS: Initially, 10 mg once daily. ideation (esp. at beginning of therapy
May increase to 20 mg/day after at least 3 or when doses are increased or de-
wks. Maximum: 20 mg once daily. Rec- creased), social interaction, mania,
ommended: 10 mg once daily. panic attacks.
Generalized Anxiety Disorder PATIENT/FAMILY TEACHING
PO: ADULTS: Initially, 10 mg
once daily • Do not stop taking medication or in-
in morning or evening. May increase crease dosage. • Avoid alcohol. • Avoid
to 20 mg after minimum of 1 wk. tasks that require alertness, motor skills
ELDERLY: 10 mg/day. until response to drug is established.
• Report worsening depression, suicidal
Dosage in Renal Impairment ideation, unusual changes in behavior.
Mild to moderate impairment: No
dose adjustment. Severe impairment:
Use caution in pts with CrCl less than
20 mL/min. esmolol
Dosage in Hepatic Impairment es-moe-lol
10 mg/day. (Brevibloc)
Do not confuse Brevibloc with
SIDE EFFECTS Bumex or Buprenex, or esmolol
Frequent (21%–11%): Nausea, dry mouth, with Osmitrol.
drowsiness, insomnia, diaphoresis.
Occasional (8%–4%): Tremor, diar- uCLASSIFICATION
rhea, abnormal ejaculation, dyspepsia, PHARMACOTHERAPEUTIC: Beta 1 -
fatigue, anxiety, vomiting, anorexia. Rare adrenergic blocker. CLINICAL: Anti-
(3%–2%): Sinusitis, sexual dysfunction, arrhythmic, antihypertensive.

underlined – top prescribed drug


esmolol 453

USES pamil), dronedarone, rivastigmine


Rapid, short-term control of ventricular may increase the bradycardic effect.
rate in supraventricular tachycardia (SVT), May increase bradycardic effect of fin-
atrial fibrillation or flutter; treatment of golimod. May increase vasoconstrict-
tachycardia and/or hypertension (esp. ing effect of ergot derivatives (e.g.,
intraop or postop). Treatment of noncom- ergotamine). HERBAL: Herbals with
pensatory sinus tachycardia. OFF-LABEL: hypotensive properties (e.g., garlic,
Postoperative hypertension or SVT in chil- ginger, gingko biloba) may increase E
dren. Arrhythmia and/or rate control in effect. Herbals with hypertensive
ACS, intubation, thyroid storm, pheochro- properties (e.g., yohimbe) may
mocytoma, electroconvulsive therapy. decrease effect. FOOD: None known. LAB
VALUES: None significant.
PRECAUTIONS
AVAILABILITY (Rx)
Contraindications: Hypersensitivity to
esmolol. Cardiogenic shock, uncompen- 10 mg/mL (10 mL,
Injection Solution:
sated cardiac failure, second- or third- 250 mL), 20 mg/mL (100 mL).
degree heart block (except in pts with
ADMINISTRATION/HANDLING
pacemaker), severe sinus bradycardia,
sick sinus syndrome, IV administration b ALERT c Give by IV infusion. Avoid
of calcium blockers in close proximity to butterfly needles, very small veins (can
esmolol, pulmonary hypertension. Cau- cause thrombophlebitis).
tions: Compensated HF; concurrent use IV
of digoxin, verapamil, dilTIAZem. Diabe-
tes, myasthenia gravis, renal impairment, Rate of administration • Administer
history of anaphylaxis to allergens. Hypo- by controlled infusion device; titrate to
volemia, hypertension, bronchospastic tolerance and response. • Infuse IV
disease, peripheral vascular disease, loading dose over 1–2 min. • Hypoten-
Raynaud’s disease. sion (systolic B/P less than 90 mm Hg) is
greatest during first 30 min of IV infu-
ACTION sion.
Selectively blocks beta1-adrenergic recep- Storage • Use only clear and colorless
tors. Therapeutic Effect: Slows sinus to light yellow solution. • Discard solu-
heart rate, decreases cardiac output, tion if discolored or precipitate forms.
reducing B/P.
IV INCOMPATIBILITIES
PHARMACOKINETICS Amphotericin B complex (Abelcet,
Rapidly metabolized primarily by ester- AmBisome, Amphotec), furosemide
­
ase in cytosol of red blood cells. Protein (Lasix).
binding: 55%. Less than 1%–2% excreted
in urine. Half-life: 9 min. IV COMPATIBILITIES
Amiodarone (Cordarone), dexmedeto-
LIFESPAN CONSIDERATIONS midine (Precedex), dilTIAZem (Cardi-
Pregnancy/Lactation: Crosses placenta; zem), DOPamine (Intropin), heparin,
distributed in breast milk. Children: Safety magnesium, midazolam (Versed), potas-
and efficacy not established. Elderly: No sium chloride, propofol (Diprivan).
age-related precautions noted.
INDICATIONS/ROUTES/DOSAGE
INTERACTIONS Rate Control in Supraventricular
DRUG: Alpha-2 agonists (e.g., nor- Arrhythmias
epinephrine), calcium channel IV: ADULTS, ELDERLY: Initially, load-
blockers (e.g., dilTIAZem, vera- ing dose of 500 mcg/kg/min for 1 min,
Canadian trade name Non-Crushable Drug High Alert drug
454 esomeprazole
followed by 50 mcg/kg/min for 4 min. INTERVENTION/EVALUATION
If optimum response is not attained Monitor B/P for hypotension, ECG, heart
in 5 min, give second loading dose of rate, respiratory rate, development of
500 mcg/kg/min for 1 min, followed by diaphoresis, dizziness (usually first sign
infusion of 100 mcg/kg/min for 4 min. of impending hypotension). Assess pulse
A third (and final) loading dose can be for quality, irregular rate, bradycardia,
given and infusion increased by 50 mcg/ extremities for coldness. Assist with am-
E kg/min, up to 200 mcg/kg/min, for 4 bulation if dizziness occurs. Assess for
min. Once desired response is attained, nausea, diaphoresis, headache, fatigue.
increase infusion by no more than 25
mcg/kg/min. Infusion usually adminis-
tered over 24–48 hrs in most pts. Range:
50–200 mcg/kg/min (average dose 100 esomeprazole
mcg/kg/min).
es-o-mep-ra-zole
Intraop/Postop Tachycardia Hypertension (NexIUM, NexIUM 24 HR, Nexium
(Immediate Control) IV)
IV: ADULTS, ELDERLY: Initially, 1,000 Do not confuse esomeprazole
mcg/kg over 30 sec, then 150 mcg/kg/ with ARIPiprazole or omepra-
min infusion up to 300 mcg/kg/min. zole, or NexIUM with NexAVAR.
Dosage in Renal/Hepatic Impairment FIXED-COMBINATION(S)
No dose adjustment.
Vimovo: esomeprazole/naproxen
SIDE EFFECTS (NSAID): 20 mg/375 mg, 20 mg/500
Generally well tolerated, with transient, mg.
mild side effects. Frequent: Hypoten- uCLASSIFICATION
sion (systolic B/P less than 90 mm Hg)
manifested as dizziness, nausea, diapho- PHARMACOTHERAPEUTIC: Proton
resis, headache, cold extremities, fatigue. pump inhibitor. CLINICAL: Gastric
Occasional: Anxiety, drowsiness, flushed
acid inhibitor.
skin, vomiting, confusion, inflammation
at injection site, fever.
USES
ADVERSE EFFECTS/TOXIC PO: Short-term treatment (4–8 wks)
REACTIONS of erosive esophagitis; maintenance
Overdose may produce profound hypo- treatment of healing of erosive esopha-
tension, bradycardia, dizziness, syncope, gitis; symptomatic gastroesophageal
drowsiness, breathing difficulty, bluish reflux disease (GERD). Treatment of
fingernails or palms of hands, seizures. pathologic hypersecretory conditions,
May potentiate insulin-induced hypogly- including Zollinger-Ellison syndrome.
cemia in diabetic pts. Used in triple therapy with amoxicillin
and clarithromycin for treatment of H.
NURSING CONSIDERATIONS pylori infection in pts with duodenal
BASELINE ASSESSMENT ulcer. Reduces risk of NSAID-induced
Assess B/P, apical pulse immediately gastric ulcer. OTC: Treatment of fre-
before drug is administered (if pulse is quent heartburn (2 or more days/wk).
60 or less/min or systolic B/P is 90 mm IV: Treatment of GERD with erosive
Hg or less, withhold medication, contact esophagitis. Reduce risk of ulcer re-
physician). bleeding postprocedures.

underlined – top prescribed drug


esomeprazole 455

PRECAUTIONS ADMINISTRATION/HANDLING
Contraindications: Hypersensitivity to IV
esomeprazole, other proton pump inhibi-
tors. Cautions: May increase risk of hip, Reconstitution • For IV push, add 5
wrist, spine fractures; hepatic impair- mL of 0.9% NaCl to esomeprazole vial.
ment; elderly; Asian populations. Con- Infusion • For IV infusion, dissolve
current use of CYP3A4 inducers (e.g., contents of one vial in 50 mL 0.9% NaCl,
rifAMPin). or D5W. E
Rate of administration • For IV
ACTION push, administer over not less than 3
Inhibits H+/K+-ATPase on surface of min. For intermittent infusion (piggy-
gastric parietal cells. Therapeutic back) infuse over 10–30 min. • Flush
Effect: Reduces gastric acid secretion. line with 0.9% NaCl, or D5W, both before
and after administration.
PHARMACOKINETICS Storage • Use only clear and colorless
Well absorbed after PO administra- to very slightly yellow solution. • Dis-
tion. Protein binding: 97%. Extensively card solution if particulate forms. • IV
metabolized in liver. Primarily excreted infusion stable for 12 hrs in 0.9% NaCl or
in urine. Half-life: 1–1.5 hrs. lactated Ringer’s; 6 hrs in D5W.

LIFESPAN CONSIDERATIONS PO (Capsules)


Pregnancy/Lactation: Unknown if • Give 1 hr or more before eating (best
drug crosses placenta or is distributed before breakfast). • Do not crush, cut
in breast milk. Children: Safety and effi- capsule; administer whole. • For pts
cacy not established. Elderly: No age- with difficulty swallowing capsules, open
related precautions noted. capsule and mix pellets with 1 tbsp ap-
plesauce. Swallow immediately without
INTERACTIONS chewing.
DRUG: May decrease concentration/ PO (Oral Suspension)
effect of acalabrutinib, cefuroxime, • Empty contents into 5 mL water for
erlotinib, neratinib, pazopanib. 2.5 mg, 5 mg; 15 mL for 10 mg, 20 mg,
Strong CYP2C19 inducers (e.g., 40 mg and stir. • Let stand 2–3 min to
FLUoxetine) may decrease concen- thicken. • Stir and drink within 30 min.
tration/effect. CYP3A4 inducers
(e.g., carBAMazepine, phenytoin, IV INCOMPATIBILITIES
rifAMPin) may decrease concentra- Do not mix esomeprazole with any other
tion/effect. HERBAL: St. John’s wort medications through the same IV line or
may decrease concentration/effect. tubing.
FOOD: None known. LAB VALUES: None
significant. IV COMPATIBILITIES
AVAILABILITY (Rx) Ceftaroline (Teflaro), doripenem
(Doribax).
Injection, Powder for Reconstitu-
tion: 20 mg, 40 mg. Oral Suspension, INDICATIONS/ROUTES/DOSAGE
­Delayed-Release Packets: 2.5 mg, 5 mg,
Erosive Esophagitis
10 mg, 20 mg, 40 mg. PO: ADULTS, ELDERLY, CHILDREN 12 YRS
Capsules (Delayed-Release: [Nex- AND OLDER: 20–40 mg once daily for
IUM]): 20 mg, 40 mg. [Nexium 24 HR]: 20 4–8 wks. May continue for additional
mg. Tablets: (Delayed-Release): 20 mg. 4–8 wks. CHILDREN 1–11 YRS, WEIGHING 20
KG OR MORE: 10–20 mg/day for up to 8

Canadian trade name Non-Crushable Drug High Alert drug


456 estradiol
wks. WEIGHING LESS THAN 20 KG: 10 mg/ SIDE EFFECTS
day for up to 8 wks. CHILDREN 1–11 MOS, Frequent (7%): Headache. Occasional
WEIGHING MORE THAN 7.5 KG–12 KG: 10 (3%–2%): Diarrhea, abdominal pain, nau-
mg/day for up to 6 wks. 6–7.5 KG: 5 mg/ sea. Rare (less than 2%): Dizziness, asthe-
day for up to 6 wks. 3–5 KG: 2.5 mg/day nia, vomiting, constipation, rash, cough.
for up to 6 wks.
ADVERSE EFFECTS/TOXIC
E Maintenance Therapy for Erosive REACTIONS
Esophagitis
Pancreatitis, hepatotoxicity, interstitial
PO: ADULTS, ELDERLY: 20 mg/day.
nephritis occur rarely.
Treatment of NSAID-Induced Gastric Ulcers
PO: ADULTS, ELDERLY: 20 mg/day for 8
NURSING CONSIDERATIONS
wks. BASELINE ASSESSMENT
Assess epigastric/abdominal pain. Ques-
Prevention of NSAID-Induced Gastric
tion history of hepatic impairment,
Ulcer
pathologic bone fractures.
PO: ADULTS, ELDERLY: 20–40 mg once
daily for up to 6 mos. INTERVENTION/EVALUATION
Evaluate for therapeutic response (relief
Gastroesophageal Reflux Disease (GERD)
of GI symptoms). Question if GI discom-
IV: ADULTS, ELDERLY: 20 or 40 mg once
fort, nausea, diarrhea occur. Monitor for
daily for up to 10 days. CHILDREN 1–17
occult blood, observe for hemorrhage in
YRS, WEIGHING 55 KG OR MORE: 20 mg
pts with peptic ulcer.
once daily; 1–17 YRS, WEIGHING LESS THAN
55 KG: 10 mg once daily; 1 MO TO LESS PATIENT/FAMILY TEACHING
THAN 1 YR: 0.5 mg/kg once daily. • Report headache. • Take at least 1
PO: ADULTS, ELDERLY, CHILDREN, 12–17 hr before eating. • If swallowing cap-
YRS: 20 mg once daily for up to 8 wks. sules is difficult, open capsule and mix
CHILDREN 1–11 YRS: 10 mg/day for up to pellets with 1 tbsp applesauce. Swallow
8 wks. immediately without chewing.
Zollinger-Ellison Syndrome
PO: ADULTS, ELDERLY: 40 mg 2 times/
day. Doses up to 240 mg/day have been estradiol
used.
es-tra-dye-ole
Duodenal Ulcer Caused by Helicobacter (Alora, Climara, Delestrogen, Depo-
Pylori Estradiol, Divigel, Elestrin, Estrogel,
PO: ADULTS, ELDERLY: 20-40 mg twice Evamist, Femring, Menostar, Mini-
daily (as part of multidrug regimen). velle, Vivelle-Dot)
j BLACK BOX ALERT jIncreased
Heartburn (OTC) risk of dementia when given to
PO: ADULTS, ELDERLY: 20 mg/day for 14 women 65 yrs and older. Use of es-
days. May repeat after 4 mos if needed. trogen without progestin increases
risk of endometrial cancer in
Dosage in Renal Impairment postmenopausal women with intact
uterus. Increased risk of invasive
No dose adjustment. breast cancer in postmenopausal
women using conjugated estrogens
Dosage in Hepatic Impairment with medroxyPROGESTERone. Do
Mild to moderate impairment: No not use to prevent cardiovascular
dose adjustment. Severe impairment: disease or dementia.
Doses should not exceed 20 mg/day.

underlined – top prescribed drug


estradiol 457
Do not confuse Alora with triosis, severe hypocalcemia, hyperlipid-
Aldara, or Estraderm with emias, asthma, epilepsy, migraines, SLE,
Testoderm. hypertension, hypocalcemia, hypothy-
roidism, history of jaundice due to past
FIXED-COMBINATION(S) estrogen use or pregnancy, cardiovas-
Activella: estradiol/norethindrone cular disease, obesity, porphyria, severe
(hormone): 1 mg/0.5 mg. Climara hypocalcemia.
PRO: estradiol/levonorgestrel (pro- E
gestin): 0.045 mg/24 hr, 0.015 mg/24 ACTION
hr. Combi-patch: estradiol/norethin- Modulates pituitary secretion of gonado-
drone (hormone): 0.05 mg/0.14 mg, tropins; follicle-stimulating hormone
0.05 mg/0.25 mg. Femhrt: estradiol/ (FSH), luteinizing hormone (LH). Thera-
norethindrone (hormone): 5 mcg/1 peutic Effect: Promotes normal growth/
mg. Lunelle: estradiol/medroxy- development of female sex organs.
progesterone (progestin): 5 mg/25 mg Reduces elevated levels of FSH, LH.
per 0.5 mL.
PHARMACOKINETICS
uCLASSIFICATION Well absorbed from GI tract. Widely
PHARMACOTHERAPEUTIC: Estrogen distributed. Protein binding: 50%–80%.
derivative. CLINICAL: Estrogen, anti- Metabolized in liver. Primarily excreted
neoplastic. in urine. Half-life: Unknown.
LIFESPAN CONSIDERATIONS
USES Pregnancy/Lactation: Contraindi-
Treatment of moderate to severe vaso- cated during pregnancy. Breastfeeding
motor symptoms associated with not recommended. Children: Caution
menopause, vulvar and vaginal atrophy in pts for whom bone growth is not
associated with menopause, hypoestro- complete (may accelerate epiphyseal
genism (due to castration, hypogonad- closure). Elderly: May increase risk of
ism, primary ovarian failure), metastatic new-onset dementia.
breast cancer (palliation) in men and
postmenopausal women, advanced pros- INTERACTIONS
tate cancer (palliation), prevention of DRUG: CYP3A4 inducers (e.g., car-
osteoporosis in postmenopausal women. BAMazepine, rifAMPin) may decrease
concentration/effects. CYP3A4 inhibi-
PRECAUTIONS tors (e.g., clarithromycin, keto-
Contraindications: Hypersensitivity to es­­ conazole, ritonavir) may increase
tradiol, angioedema, hepatic dysfunction concentration/effect. May decrease
or disease, undiagnosed abnormal vagi- therapeutic effect of anastrozole,
nal bleeding, active or history of arterial exemestane. HERBAL: Herbals with
thrombosis, estrogen-dependent cancer estrogenic properties (e.g., dong
(known, suspected, or history of), known quai, ginkgo biloba, ginseng, red
or suspected breast cancer (except clover) may increase adverse effects.
for pts being treated for metastatic dis- St. John’s wort may decrease concen-
ease), pregnancy, thrombophlebitis or tration/effects of estrogens. FOOD: None
thromboembolic disorders (current or known. LAB VALUES: May increase
history of), known protein C, protein S, serum glucose, calcium, HDL, triglycer-
antithrombin deficiency or other known ides. May decrease serum cholesterol,
thrombophilic disorder. Cautions: Renal LDL. May affect metapyrone testing, thy-
insufficiency, diabetes mellitus, endome- roid function tests.

Canadian trade name Non-Crushable Drug High Alert drug


458 estradiol

AVAILABILITY (Rx) Vaginal


Cream, Topical: 0.4%, 0.6%. Emulsion,
• Apply at bedtime for best absorp-
Topical: (Estrasorb): 4.35 mg estradiol/1.74
tion. • Insert end of filled applicator
g pouch (contents of 2 pouches deliver into vagina, directed slightly toward sa-
estradiol 0.05 mg/day). Gel, Topical: crum; push plunger down com-
(Divigel): 0.1% (0.25-g packet delivers
pletely. • Avoid skin contact with cream
estradiol 0.25 mg, 0.5-g packet delivers (prevents skin absorption).
E estradiol 0.5 mg, 1-g packet delivers 1 mg). INDICATIONS/ROUTES/DOSAGE
(Elestrin): 0.06% delivers 0.52 mg estra-
Prostate Cancer
diol/actuation. (Estrogel): 0.06% delivers
0.75 mg/actuation. Injection (Cypionate): IM: (Delestrogen): ADULTS, ELDERLY: 30
Depo-Estradiol: 5 mg/mL. (Valerate): Deles-
mg or more q1–2wks.
trogen: 10 mg/mL, 20 mg/mL, 40 mg/mL.
PO: ADULTS, ELDERLY: 1–2 mg tid for at
Tablets: 0.5 mg, 1 mg, 2 mg. Topical Spray:
least 3 mos.
(Evamist): 1.53 mg/spray. Transdermal Sys- Breast Cancer (Metastatic)
tem: (Alora): twice wkly: 0.025 mg/24 hrs, PO: ADULTS, ELDERLY: 10 mg 3 times/
0.05 mg/24 hrs, 0.075 mg/24 hrs, 0.1 mg/24 day for at least 3 mos.
hrs. (Climara): once wkly: 0.025 mg/24 hrs,
0.0375 mg/24 hrs, 0.05 mg/24 hrs, 0.06 Osteoporosis Prophylaxis in
mg/24 hrs, 0.075 mg/24 hrs, 0.1 mg/24 Postmenopausal Females
hrs. (Menostar): once wkly: 0.014 mg/24 PO: ADULTS, ELDERLY: 0.5 mg/day cycli-
hrs. (Minivelle, Vivelle-Dot): twice wkly: cally (3 wks on, 1 wk off).
0.025 mg/24 hrs, 0.0375 mg/24 hrs, 0.05 Transdermal: (Climara): ADULTS,
mg/24 hrs, 0.075 mg/24 hrs, 0.1 mg/24 hrs. ELDERLY: Initially, 0.025 mg/24 hrs wkly;
Vaginal Cream: (Estrace): 0.1 mg/g. Vaginal adjust dose as needed.
Ring: (Estring): 2 mg (releases 7.5 mcg/ Transdermal: (Alora, Minivelle,
day over 90 days). (Femring): 0.05 mg/day Vivelle-Dot): ADULTS, ELDERLY: Initially,
(total estradiol 12.4 mg release 0.05 mg/ 0.025 mg/24 hrs patch twice wkly; adjust
day over 3 mos); 0.1 mg/day (total estradiol dose as needed.
24.8 mg-release 0.1 mg/day over 3 mos). Transdermal: (Menostar): ADULTS,
Vaginal Tablet: (Vagifem): 10 mcg. ELDERLY: 0.014 mg/24 hrs patch wkly.
ADMINISTRATION/HANDLING Female Hypoestrogenism
IM PO: ADULTS, ELDERLY: 1–2 mg/day;
• Rotate vial to disperse drug in solu- adjust dose as needed.
tion. • Inject deep IM in large muscle IM: (Depo-Estradiol): ADULTS, ELDERLY:
mass. 1.5–2 mg monthly.
IM: (Delestrogen): ADULTS, ELDERLY:
PO 10–20 mg q4wks.
• Administer at same time each day. Transdermal: (Alora): Initially, 0.05
• Administer with food. mg/day twice wkly. (Climara): 0.025 mg/
day once wkly. (Vivelle-Dot): 0.025 mg/
Transdermal day twice wkly.
• Remove old patch; select new site (but-
tocks are alternative application Vasomotor Symptoms Associated with
site). • Peel off protective strip to expose Menopause
adhesive surface. • Apply to clean, dry, PO: ADULTS, ELDERLY: 1–2 mg/day
intact skin on trunk of body (area with as cyclically (3 wks on, 1 wk off); adjust
little hair as possible). • Press in place dose as needed.
for at least 10 sec (do not apply to breasts IM: (Depo-Estradiol): ADULTS, ELDERLY:
or waistline). 1–5 mg q3–4wks.

underlined – top prescribed drug


estradiol 459
IM: (Delestrogen): ADULTS, ELDERLY: SIDE EFFECTS
10–20 mg q4wks. Frequent: Anorexia, nausea, swelling
Topical emulsion: (Estrasorb): ADULTS, of breasts, peripheral edema marked
ELDERLY: 3.48 g (contents of 2 pouches) by swollen ankles and feet. Transder-
once daily in the morning. mal: Skin irritation, redness. Occa-
Topical gel: (Estrogel): ADULTS, sional: Vomiting (esp. with high doses),
ELDERLY: 1.25 g/day. headache (may be severe), intolerance
Transdermal spray: (Evamist): Ini- to contact lenses, hypertension, glucose E
tially, 1 spray daily. May increase to 2–3 intolerance, brown spots on exposed
sprays daily. skin. Vaginal: Local irritation, vaginal
Transdermal: (Climara): ADULTS, discharge, changes in vaginal bleed-
ELDERLY: 0.025 mg/24 hrs wkly. Adjust ing (spotting, breakthrough, prolonged
dose as needed. bleeding). Rare: Chorea (involuntary
Transdermal: ADULTS, ELDERLY: (Alora): movements), hirsutism (abnormal hairi-
0.05 mg/24 hrs twice wkly. (Vivelle- ness), loss of scalp hair, depression.
Dot): 0.0375 mg/24 hrs twice wkly.
Vaginal ring: (Femring): ADULTS, ADVERSE EFFECTS/TOXIC
ELDERLY: 0.05 mg. May increase to 0.1 REACTIONS
mg if needed. Prolonged administration increases risk
of gallbladder disease, thromboembolic
Vulvar and Vaginal Atrophy Associated
disease, breast/cervical/vaginal/endo-
with Menopause
metrial/hepatic carcinoma. Cholestatic
IM: (Delestrogen): ADULTS, EL­DER­
jaundice occurs rarely.
­LY: 10–20 mg q4wks.
Vaginal ring: (Femring): Initially 0.05 NURSING CONSIDERATIONS
mg. Usual dose: 0.05–0.1 mg q3mos.
PO: (Estrace): 1–2 mg/day 3 wks on and BASELINE ASSESSMENT
1 wk off. Assess frequency/severity of vasomotor
Topical gel: (Estrogel): 1.25 g/day at symptoms. Question medical history
same time each day. as listed in Precautions. Question for
Transdermal: (Alora, Climara, Viv- possibility of pregnancy (contraindi-
elle-Dot): See dose in availability sec- cated).
tion).
Vaginal ring: (Estring): ADULTS,
INTERVENTION/EVALUATION
ELDERLY: 2 mg. Ring to remain in place Monitor B/P, weight, serum calcium,
for 90 days. glucose, LFT. Monitor for loss of vision,
Vaginal cream: (Estrace): Insert 2–4 sudden onset of proptosis, diplopia, mi-
g/day intravaginally for 2 wks, then graine, thromboembolic disorders.
reduce dose to half of initial dose for 2 PATIENT/FAMILY TEACHING
wks, then maintenance dose of 1 g 1–3
times/wk. • Limit alcohol, caffeine. • Avoid
Vaginal tablet: (Vagifem): ADULTS, grapefruit products. • Immediately re-
Initially, 1 tablet/day for 2 wks.
ELDERLY:
port sudden headache, vomiting, distur-
Maintenance: 1 tablet twice wkly. bance of vision/speech, numbness/weak-
ness of extremities, chest pain, calf pain,
Dosage in Renal Impairment shortness of breath, severe abdominal
No dose adjustment. pain, mental depression, unusual bleed-
ing. • Avoid smoking. • Report ab-
Dosage in Hepatic Impairment normal vaginal bleeding. • Never place
Contraindicated. patch on breast or waistline.

Canadian trade name Non-Crushable Drug High Alert drug


460 eszopiclone
may increase concentration/toxicity. Strong
eszopiclone CYP3A4 inducers (e.g., carBAMaze-
pine, phenytoin, rifAMPin) may decrease
e-zop-i-klone concentration/effect. CNS depressants
(Lunesta) (e.g., alcohol, morphine, oxyCODONE,
Do not confuse Lunesta with zolpidem) may increase CNS depression.
Neulasta. HERBAL: Herbals with sedative prop-
E erties (e.g., chamomile, kava kava,
uCLASSIFICATION
valerian) may increase CNS depression.
PHARMACOTHERAPEUTIC: Non- St. John’s wort may decrease concentra-
benzodiazepine (Schedule IV). CLIN- tion/effect. FOOD: Onset of action may be
ICAL: Hypnotic. reduced if taken with or immediately after a
high-fat meal. LAB VALUES: None known.
USES AVAILABILITY (Rx)
Treatment of insomnia.
Tablets, Film-Coated: 1 mg, 2 mg, 3
PRECAUTIONS mg.
Contraindications: Hypersensitivity to eszop- ADMINISTRATION/HANDLING
iclone. Cautions: Hepatic impairment, com-
PO
promised respiratory function, COPD, sleep
• Should be administered immediately
apnea, clinical depression, suicidal ideation,
before bedtime. • Do not give with or
history of drug dependence; concomitant
immediately following a high-fat or heavy
CNS depressants, strong CYP3A4 inhibitors
meal. • Do not break, crush, dissolve,
(e.g., ketoconazole); elderly.
or divide tablet.
ACTION
INDICATIONS/ROUTES/DOSAGE
May interact with GABA-receptor com-
Insomnia
plexes at binding domains located close
PO: ADULTS: 1 mg before bedtime.
to or allosterically coupled to benzo-
Maximum: 3 mg. Concurrent use
diazepine receptors. Therapeutic
with CYP3A4 inhibitors (e.g., clar-
Effect: Prevents insomnia, difficulty
ithromycin, erythromycin, azole
maintaining normal sleep.
antifungals): 1 mg before bedtime; if
PHARMACOKINETICS needed, dose may be increased to 2 mg.
ELDERLY, DEBILITATED PTS: Initially, 1 mg
Rapidly absorbed following PO admin-
before bedtime. Maximum: 2 mg.
istration. Protein binding: 52%–59%.
Metabolized in liver. Excreted in urine. Sleep Maintenance Difficulty
Half-life: 5–6 hrs. PO: ADULTS: 2 mg before bedtime.
LIFESPAN CONSIDERATIONS Dosage in Renal Impairment
Pregnancy/Lactation: Unknown if No dose adjustment.
drug crosses placenta or is distributed
in breast milk. Children: Safety and Dosage in Hepatic Impairment
efficacy not established. Elderly: Pts Use caution. Initially, 1 mg immediately
with impaired motor or cognitive perfor- before bedtime. Maximum: 2 mg.
mance may require dosage adjustment. SIDE EFFECTS
INTERACTIONS Frequent (34%–21%): Unpleasant taste,
headache. Occasional (10%–4%): Drows-
DRUG: CYP3A4 inhibitors (e.g., clar-
iness, dry mouth, dyspepsia, dizziness,
ithromycin, ketoconazole, ritonavir)

underlined – top prescribed drug


etanercept 461
nervousness, nausea, rash, pruritus, Do not confuse Enbrel with
depression, diarrhea. Rare (3%–2%): Hal- Levbid.
lucinations, anxiety, confusion, abnormal
dreams, decreased libido, neuralgia. uCLASSIFICATION
PHARMACOTHERAPEUTIC: Protein,
ADVERSE EFFECTS/TOXIC TNF inhibitor. CLINICAL: Antiarthritic.
REACTIONS
Chest pain, peripheral edema occur E
occasionally. USES
Treatment of moderate to severely active
NURSING CONSIDERATIONS rheumatoid arthritis (RA). Treatment of
BASELINE ASSESSMENT
moderately to severely active polyarticular
juvenile idiopathic arthritis (JIA), anky-
Assess B/P, pulse, respirations. Raise bed losing spondylitis (AS), psoriatic arthritis.
rails, provide call light. Provide environment Treatment of chronic, moderate to severe
conducive to sleep (quiet environment, low plaque psoriasis. OFF-LABEL: Treatment
or no lighting). Question usual sleep pat- of acute graft-versus-host disease.
terns. Initiate fall precautions. Screen for
other conditions affecting sleep (e.g., stress, PRECAUTIONS
depression, hyperactivity, drug abuse). Contraindications: Hypersensitivity to
INTERVENTION/EVALUATION etanercept. Serious active infection or
Assess sleep pattern of pt. Evaluate for sepsis. Cautions: History of recurrent
therapeutic response (decrease in num- infections, illnesses that predispose to
ber of nocturnal awakenings, increase in infection (e.g., diabetes, travel from
length of sleep). areas of endemic mycosis). History of
HF, decreased left ventricular function,
PATIENT/FAMILY TEACHING significant hematologic abnormalities;
• Take only when experiencing insom- moderate to severe alcoholic hepatitis,
nia. Do not take when insomnia is not elderly, preexisting or recent-onset CNS
present. • Do not break, chew, crush, demyelinating disorder.
dissolve, or divide tablet. Take
whole. • Avoid alcohol. • At least 8 ACTION
hrs must be devoted for sleep time before Binds to tumor necrosis factor (TNF),
daily activity begins. • Take immedi- blocking its interaction with cell surface
ately before bedtime. • Report insom- receptors. Elevated levels of TNF, involved
nia that worsens or persists longer than in inflammatory processes and the
7–10 days, abnormal thoughts or behav- resulting joint pathology of rheumatoid
ior, memory loss, anxiety. arthritis, JIA, AS, and plaque psoriasis.
Therapeutic Effect: Relieves symp-
toms of arthritis, psoriasis, spondylitis.

etanercept PHARMACOKINETICS
Well absorbed after SQ administration.
e-tan-er-sept Half-life: 72–132 hrs.
(Enbrel, Enbrel SureClick, Enbrel Mini)
LIFESPAN CONSIDERATIONS
j BLACK BOX ALERT jSerious,
potentially fatal infections, includ- Pregnancy/Lactation: Unknown if
ing bacterial sepsis, tuberculosis, distributed in breast milk. Children: No
have occurred. Lymphomas, other age-related precautions noted in pts 4 yrs
malignancies may occur (reported and older. Elderly: No age-related pre-
in children/adolescents).
cautions noted.

Canadian trade name Non-Crushable Drug High Alert drug


462 etanercept

INTERACTIONS Plaque Psoriasis


DRUG: Anakinra, anti-TNF agents, SQ: ADULTS, ELDERLY: 50 mg twice wkly
baricitinib, pimecrolimus, ritux- (give 3–4 days apart) for 3 mos. (25
imab, tacrolimus (topical), tocili- mg or 50 mg once wkly have also been
zumab may increase adverse/toxic used.) Maintenance: 50 mg once wkly.
CHILDREN 4 YRS AND OLDER WEIGHING
effects. May increase concentration,
63 KG OR MORE: 50 mg once wkly. LESS
adverse/toxic effects of belimumab,
E natalizumab, tofacitinib. Use of live THAN 63 KG: 0.8 mg/kg once wkly. Maxi-
virus vaccines may potentiate virus mum: 50 mg/wk.
replication, increase vaccine side effect, Dosage in Renal/Hepatic Impairment
decrease pt’s antibody response to vac- No dose adjustment.
cine. HERBAL: Echinacea may decrease
effects. FOOD: None known. LAB VAL- SIDE EFFECTS
UES: May increase serum alkaline phos- Frequent (37%): Injection site erythema,
phatase, ALT, AST, bilirubin. pruritus, pain, swelling; abdominal pain,
AVAILABILITY (Rx) vomiting (more common in children than
adults). Occasional (16%–4%): Head-
Injection Solution (Cartridge): 50 mg/mL. ache, rhinitis, dizziness, pharyngitis,
Injection, Solution (Prefilled Syringe): 25 cough, asthenia, abdominal pain, dys-
mg/0.5 mL, 50 mg/mL. Injection, Solu- pepsia. Rare (less than 3%): Sinusitis,
tion (Autoinjector): 50 mg/mL. Solution, allergic reaction.
Reconstituted: 25 mg.
ADVERSE EFFECTS/TOXIC
ADMINISTRATION/HANDLING REACTIONS
b ALERT c Do not add other medica- Infection (pyelonephritis, cellulitis,
tions to solution. Do not use filter during osteomyelitis, wound infection, leg ulcer,
reconstitution or administration. septic arthritis, diarrhea, bronchitis,
SQ pneumonia) occurs in 29%–38% of pts.
• Refrigerate prefilled syringes. • In- Rare adverse effects include heart failure,
ject into thigh, abdomen, upper arm. hypertension, hypotension, pancreatitis,
Rotate injection sites. • Give new injec- GI hemorrhage.
tion at least 1 inch from an old site and
NURSING CONSIDERATIONS
never into area where skin is tender,
bruised, red, hard. • Once reconsti- BASELINE ASSESSMENT
tuted, may be stored in vial for up to 14 Assess onset, type, location, duration
days refrigerated. of pain, inflammation. If significant ex-
posure to varicella virus has occurred
INDICATIONS/ROUTES/DOSAGE during treatment, therapy should be tem-
Rheumatoid Arthritis (RA), Psoriatic porarily discontinued and treatment with
Arthritis, Ankylosing Spondylitis varicella-zoster immune globulin should
SQ: ADULTS, ELDERLY: 25 mg twice wkly be considered. Screen for active infec-
given 72–96 hrs apart or 50 mg once tion. Question history as listed in Precau-
wkly. Maximum: 50 mg/wk. tions. Question travel history.
Juvenile Rheumatoid Arthritis (JIA) INTERVENTION/EVALUATION
SQ: CHILDREN 2–17 YRS: (63 kg or Assess for improvement of joint swelling,
greater): 50 mg once weekly. (Less than pain, tenderness. Monitor erythrocyte
63 kg): 0.8 mg/kg once weekly. Maxi- sedimentation rate (ESR), C-reactive
mum: 50 mg/dose. protein level, CBC with differential, plate-
let count. Observe for signs of infection.

underlined – top prescribed drug


etoposide, VP-16 463
PATIENT/FAMILY TEACHING ACTION
• Instruct pt in SQ injection technique, Induces single- and double-stranded
including areas of body acceptable as breaks in DNA. Cell cycle–dependent and
injection sites. • Injection site reac- phase-specific; most effective in S and
tion generally occurs in first mo of G2 phases of cell division. Therapeutic
treatment and decreases in frequency Effect: Inhibits, alters DNA synthesis.
during continued therapy. • Do not
receive live vaccines during treat- PHARMACOKINETICS E
ment. • Report persistent fever, bruis- Variably absorbed from GI tract. Rap-
ing, bleeding, pallor. idly distributed, low concentrations in
CSF. Protein binding: 97%. Metabolized
in liver. Primarily excreted in urine.
Not removed by hemodialysis. Half-
etoposide, VP-16 life: 3–12 hrs.
e-toe-poe-side LIFESPAN CONSIDERATIONS
(Etopophos, Toposar, VePesid ) Pregnancy/Lactation: If possible, avoid
j BLACK BOX ALERT jSevere use during pregnancy, esp. first trimester.
myelosuppression with resulting May cause fetal harm. Breastfeeding not
infection, bleeding may occur. recommended. Children: Safety and effi-
Must be administered by personnel
trained in administration/handling cacy not established. Elderly: Age-related
of chemotherapeutic agents. renal impairment may require dosage
Do not confuse etoposide with adjustment.
etidronate, or VePesid with
Pepcid or Versed. INTERACTIONS
DRUG: Bone marrow depressants
uCLASSIFICATION (e.g., cladribine) may increase myelo-
PHARMACOTHERAPEUTIC: Topoi- suppression. Live-virus vaccines may
somerase II inhibitor. CLINICAL: An- potentiate virus replication, increase vac-
tineoplastic. cine side effects, decrease pt’s antibody
response to vaccine. Strong CYP3A4
inducers (e.g., carBAMazepine,
USES phenytoin, rifAMPin) may decrease
Treatment of refractory testicular tumors, concentration/effect. HERBAL: St.
small-cell lung carcinoma. OFF-LABEL: John’s wort may decrease concentra-
Acute lymphocytic, acute nonlympho- tion. FOOD: None known. LAB VAL-
cytic leukemias; Ewing’s and Kaposi’s UES: Expected decrease of leukocytes,
sarcoma; Hodgkin’s and non-Hodgkin’s platelets, RBC, Hgb, Hct.
lymphomas; endometrial, gastric, non–
small-cell lung carcinomas; multiple AVAILABILITY (Rx)
myeloma; myelodysplastic syndromes; Capsules: 50 mg. Injection, Powder for
neuroblastoma; osteosarcoma; ovarian Reconstitution: (Etopophos): 100 mg.
germ cell tumors; primary brain, gesta- Injection Solution: (Toposar): 20 mg/mL
tional trophoblastic tumors; soft tissue (5 mL, 25 mL, 50 mL).
sarcomas; Wilms tumor.
ADMINISTRATION/HANDLING
PRECAUTIONS b ALERT c Administer by slow IV infu-
Hypersensitivity to eto-
Contraindications: sion. Wear gloves when preparing solu-
poside. Cautions:Hepatic/renal impair- tion. If powder or solution comes in
ment, myelosuppression, elderly, pts with contact with skin, wash immediately and
low serum albumin. thoroughly with soap, water. May be car-
Canadian trade name Non-Crushable Drug High Alert drug
464 etoposide, VP-16
cinogenic, mutagenic, teratogenic. Han- DAUNOrubicin (Cerubidine), DOXOru-
dle with extreme care during prepara- bicin (Adriamycin), granisetron (Kytril),
tion, administration. mitoXANTRONE (Novantrone), ondan-
IV setron (Zofran). Etopophos: CARBO-
platin (Paraplatin), CISplatin (Platinol),
Reconstitution cytarabine (Cytosar), dacarbazine (DTIC-
Toposar • Dilute to a concentra- Dome), DAUNOrubicin (Cerubidine),
E tion of 0.2–0.4 mg/mL in D5W or 0.9% dexamethasone (Decadron), diphen-
NaCl. hydrAMINE (Benadryl), DOXOrubicin
Etopophos • Reconstitute each 100 mg (Adriamycin), granisetron (Kytril), mag-
with 5–10 mL Sterile Water for Injection, nesium sulfate, mannitol, mitoXANTRONE
D5W, or 0.9% NaCl to provide concentra- (Novantrone), ondansetron (Zofran),
tion of 20 mg/mL or 10 mg/mL, respec- potassium chloride.
tively. • May give without further dilution
or further dilute to concentration as low as INDICATIONS/ROUTES/DOSAGE
0.1 mg/mL with 0.9% NaCl or D5W. b ALERT c Dosage individualized
Rate of administration • (Toposar) based on clinical response, tolerance to
Infuse slowly, at least 30–60 min (rapid adverse effects. Treatment repeated at 3-
IV may produce marked hypotension) to 4-wk intervals. Refer to individual
at a rate not to exceed 100 mg/m2/ protocols.
hr. • Monitor for anaphylactic reac-
tion during infusion (chills, fever, dys- Refractory Testicular Tumors
pnea, diaphoresis, lacrimation, sneezing, IV: ADULTS: 50–100 mg/m2/day on days
throat, back, chest pain). • (Etopo- 1–5, or 100 mg/m2/day on days 1, 3, 5
phos) May give over as little as 5 min up (as combination therapy). Give q3–4wks
to 210 min. for 3–4 courses.
Storage • (Toposar) Store injection at
room temperature before dilution. • Con- Small-Cell Lung Carcinoma
centrate for injection is clear, yellow. PO: ADULTS: Twice the IV dose rounded
• Diluted solution is stable at room tem- to nearest 50 mg. Give once daily for
perature for 96 hrs at 0.2 mg/mL, 24 hrs doses 200 mg or less, in divided doses
at 0.4 mg/mL. • Discard if crystalliza- for dosages greater than 200 mg.
tion occurs. • (Etopophos) Refrigerate IV: ADULTS: 35 mg/m2/day for 4 con-
vials. • Stable at room temperature for secutive days up to 50 mg/m2/day for 5
24 hrs or for 7 days if refrigerated after consecutive days q3–4wks (as combina-
reconstitution. tion therapy).

PO Dosage in Renal Impairment


Storage • Refrigerate gelatin capsules. Creatinine
Clearance Dosage
IV INCOMPATIBILITIES
15–50 mL/min 75% of normal dose
VePesid: Cefepime (Maxipime), filgras- Less than 15 mL/ Consider further dose
tim (Neupogen). Etopophos: Ampho- min reduction.
tericin B (Fungizone), cefepime (Maxip-
ime), chlorproMAZINE (Thorazine), Dosage in Hepatic Impairment
methylPREDNISolone (Solu-Medrol), No dose adjustment.
prochlorperazine (Compazine).
SIDE EFFECTS
IV COMPATIBILITIES Frequent (66%–43%): Mild to moderate
VePesid: CARBOplatin (Paraplatin), CIS- nausea/vomiting, alopecia. Occasional
platin (Platinol), cytarabine (Cytosar), (13%–6%): Diarrhea, anorexia, stoma-

underlined – top prescribed drug


everolimus 465
titis. Rare (2% or less): Hypotension,
peripheral neuropathy. everolimus
ADVERSE EFFECTS/TOXIC e-veer-oh-li-mus
REACTIONS (Afinitor, Afinitor Disperz, Zortress)
Myelosuppression manifested as hema- j BLACK BOX ALERT jIm-
tologic toxicity, principally anemia, munosuppressant (may result in
infection, malignancy including lym- E
leukopenia (occurring 7–14 days after phoma or skin cancer); increased
drug administration), thrombocytopenia risk of nephrotoxicity in renal
(occurring 9–16 days after administra- transplants (avoid standard doses
tion), and, to lesser extent, pancytope- of cycloSPORINE); increased risk of
nia. Bone marrow recovery occurs by renal arterial or venous thrombosis
in renal transplants.
day 20. Hepatotoxicity occurs occasion-
ally. Do not confuse Afinitor with
Lipitor, or everolimus with
NURSING CONSIDERATIONS sirolimus, tacrolimus, or tem-
sirolimus.
BASELINE ASSESSMENT
Obtain CBC before and at frequent inter- uCLASSIFICATION
vals during therapy. Antiemetics readily PHARMACOTHERAPEUTIC: mTOR
control nausea, vomiting. Offer emo- kinase inhibitor. CLINICAL: Antineo-
tional support. plastic, immunosuppressant.
INTERVENTION/EVALUATION
Monitor CBC, B/P, hepatic/renal func- USES
tion tests. Monitor daily pattern of Afinitor: Treatment of advanced renal
bowel activity, stool consistency. Moni- cell carcinoma after failure of treatment
tor for hematologic toxicity (fever, sore with SUNItinib or SORAfenib. Treatment
throat, signs of local infection, unusual of subependymal giant cell astrocytoma
bruising/bleeding from any site), symp- (SEGA) associated with tuberous scle-
toms of anemia (excessive fatigue, rosis. Treatment of progressive neuro-
weakness). Assess for paresthesia endocrine tumors of pancreatic origin
(peripheral neuropathy). Monitor for and progressive, well-differentiated, non-
stomatitis. functional neuroendocrine tumors of GI
PATIENT/FAMILY TEACHING
or lung origin. Treatment of advanced
hormone receptor–positive, HER2-neg-
• Hair loss is reversible, but new hair ative breast cancer in postmenopausal
growth may have different color, tex- women. Treatment of tuberous sclerosis
ture. • Do not have immunizations complex (TSC) not requiring immediate
without physician’s approval (drug low- surgery. Afinitor Disperz: Treatment
ers resistance). • Avoid contact with of SEGA associated with TSC requiring
those who have recently received live intervention but that cannot be curatively
virus vaccine. • Promptly report fever, resected. Treatment of TSC-associated
sore throat, signs of local infection, un- partial-onset seizures. Zortress: Pro-
usual bruising or bleeding from any phylaxis of organ rejection after kid-
site, burning or pain with urination, ney/liver transplant at low to moderate
numbness in extremities, yellowing of immunologic risk. OFF-LABEL: Relapsed
skin or eyes. or refractory Waldenström’s macro-
globulinemia. Treatment of progressive
advanced carcinoid tumors.

Canadian trade name Non-Crushable Drug High Alert drug


466 everolimus

PRECAUTIONS tion, toxicity. HERBAL: Echinacea may


Contraindications: Hypersensitivity to decrease therapeutic effect. St. John’s
everolimus, sirolimus, other rapamycin wort may decrease plasma concentra-
derivatives. Cautions: Noninfectious tion. FOOD: High-fat meals may reduce
pneumonitis; viral, fungal, or bacterial plasma concentration. Grapefruit
infection; oral ulceration; mucositis; products may increase concentration
current immunosuppression; heredi- (potential for myelotoxicity, nephrotoxic-
E tary galactose intolerance; renal/hepatic ity). LAB VALUES: May increase serum
impairment; hyperlipidemia; concurrent BUN, creatinine, glucose, triglycerides,
use of CYP3A4 inducers and inhibitors. lipids. May decrease neutrophils, Hgb,
Medications known to cause angio- platelets.
edema.
AVAILABILITY (Rx)
ACTION Tablets: (Zortress): 0.25 mg, 0.5 mg,
Binds to the FK binding protein to form 0.75 mg, 1 mg. Tablets: (Afinitor): 2.5 mg, 5
a complex that inhibits activation of mg, 7.5 mg, 10 mg. Tablets for Oral Suspen-
mTOR. Inhibits vascular endothelial sion: (Afinitor Disperz): 2 mg, 3 mg, 5 mg.
growth factor (VEGF). Therapeutic
Effect: Reduces cell proliferation, pro- ADMINISTRATION/HANDLING
duces cell death. Has antiproliferative • Give without regard to food. • Swal-
and antiangiogenic properties. low tablets whole; do not crush/cut Afini-
tor or Zortress. • If pt unable to swal-
PHARMACOKINETICS low Afinitor tablets, may disperse in
Peak concentration occurs in 1–2 hrs water with gentle stirring; give immedi-
following administration, with steady- ately. • Administer Afinitor Disperz as
state levels achieved in 2 wks. Undergoes suspension only. Disperse in water until
extensive hepatic metabolism. Protein dissolved. • Avoid direct contact of dis-
binding: 74%. Eliminated in feces (80%), persed tablet or oral solution with skin
urine (5%). Half-life: 30 hrs. or mucous membranes.
LIFESPAN CONSIDERATIONS INDICATIONS/ROUTES/DOSAGE
Pregnancy/Lactation: Avoid preg- b ALERT c If pt requires coadministra-
nancy during treatment and for up to 8 tion of a strong CYP3A4 inducer (e.g.,
wks after discontinuation. Breastfeeding carBAMazepine, dexamethasone, PHE-
not recommended during treatment and Nobarbital, phenytoin, rifabutin, ri-
for up to 2 wks after discontinuation. May fAMPin), consider doubling the dose. If
cause fetal harm. Unknown if distributed strong inducer is discontinued, reduce
in breast milk. Children: Safety and effi- everolimus to dose used prior to initia-
cacy not established. Elderly: No age- tion. If moderate CYP3A4 inhibitors are
related precautions noted. required, reduce dose by 50%.
INTERACTIONS Renal Carcinoma, Neuroendocrine
DRUG: CYP3A4 inhibitors (e.g., Tumors, Breast Cancer, TSC
clarithromycin, ketoconazole, PO: ADULTS, ELDERLY: (Afinitor): 10
ritonavir) may increase concentra- mg once daily. Coadministration with
tion. CYP3A4 inducers (e.g., carBA- CYP3A4 inhibitors or P-gp inhibi-
Mazepine, phenytoin, rifAMPin) tors: 2.5 mg once daily. May increase
may decrease concentration. P-gp to 5 mg/day. Coadministration with
inhibitors (e.g., cycloSPORINE) CYP3A4 inducers: Increase by 5-mg
may increase everolimus concentra- increments up to 20 mg/day.

underlined – top prescribed drug


everolimus 467
Renal Transplant Rejection Prophylaxis SIDE EFFECTS
PO: ADULTS, ELDERLY: (Zortress): Ini-
Common (44%–26%): Stomatitis, asthenia.
tially, 0.75 mg 2 times/day. Adjust dose Diarrhea, cough, rash, nausea. Frequent
at 4- to 5-day intervals based on serum (25%–20%): Peripheral edema, anorexia,
concentration, tolerability, and response. dyspnea, vomiting, pyrexia. Occasional
Give in combination with basiliximab (19%–10%): Mucosal inflammation, head-
and concurrently with reduced doses of ache, epistaxis, pruritus, dry skin, epi-
cycloSPORINE and corticosteroids. gastric distress, extremity pain. Rare (less E
Liver Transplant Rejection Prophylaxis than 10%): Abdominal pain, insomnia,
(begin at least 30 days post-transplant) dry mouth, dizziness, paresthesia, eyelid
PO: ADULTS, ELDERLY: (Zortress): Ini- edema, hypertension, nail disorder, chills.
tially, 1 mg 2 times/day. Adjust dose at ADVERSE EFFECTS/TOXIC
4- to 5-day intervals based on serum REACTIONS
concentration, tolerability, and response.
Noninfectious pneumonitis character-
SEGA ized as hypoxia, pleural effusion, cough,
PO: ADULTS, ELDERLY: Initially, 4.5 mg/m2 or dyspnea was reported in 14% of pts;
once daily, titrated to attain trough concen- Grade 3 noninfectious pneumonitis
tration of 5–15 ng/mL. If trough greater reported in 4%. Localized and systemic
than 15 ng/mL: reduce dose by 2.5 mg/ infections, including pneumonia, other
day (tablets) or 2 mg/day (tablets for oral bacterial infections, and invasive fungal
suspension). If trough less than 15 ng/ infections, have occurred due to evero-
mL: increase dose by 2.5 mg/day (tablets) limus immunosuppressive properties.
or 2 mg/day (tablets for oral suspension). Renal failure occurs in 3% of pts.

Tsc-Associated Partial-Onset Seizures NURSING CONSIDERATIONS


PO: ADULTS, ELDERLY, CHILDREN 2 YRS
BASELINE ASSESSMENT
AND OLDER: Initially, 5 mg/m2 once daily,
titrated to attain trough concentration of Assess medical history, esp. renal func-
5–15 ng/mL. Maximum dose increment tion, use of other immunosuppressants.
at any titration must not exceed 5 mg. Obtain CBC, BMP, LFT before treatment
begins and routinely thereafter. Offer
Dosage in Renal Impairment emotional support.
No dose adjustment. INTERVENTION/EVALUATION
Dosage in Hepatic Impairment Offer antiemetics to control nausea,
Mild Moderate Severe vomiting. Monitor daily pattern of bowel
Breast 7.5 mg/ 5 mg/day 2.5 mg/ activity, stool consistency. Assess skin for
Cancer day or or 2.5 day evidence of rash, edema. Monitor CBC,
PNET, 5 mg/ mg/day particularly Hgb, platelet, neutrophil
RCC, re- day count; BUN, creatinine, LFT. Monitor for
nal an- shortness of breath, fatigue, hypertension.
giomyo- Assess mouth for stomatitis, mucositis.
lipoma
Liver/­ Reduce Reduce Reduce PATIENT/FAMILY TEACHING
Renal dose dose by dose by • Take dose at same time each
trans- by 33% 50% 50%
plant
day. • Avoid crowds, those with known
SEGA No No Initial infection. • Avoid contact with anyone
change change dose who recently received live virus vac-
2.5 mg/ cine. • Do not have immunizations
m2/day without physician’s approval (drug low-

Canadian trade name Non-Crushable Drug High Alert drug


468 exemestane
ers body resistance). • Promptly report PHARMACOKINETICS
fever, unusual bruising/bleeding from Rapidly absorbed after PO administra-
any site. • Avoid direct contact of tion. Protein binding: 90%. Distributed
crushed tablets with skin or mucous extensively into tissues. Metabolized in
membrane (wash thoroughly if contact liver. Excreted in urine and feces. Half-
occurs). • Avoid grapefruit products. life: 24 hrs.
E LIFESPAN CONSIDERATIONS
exemestane Pregnancy/Lactation: Indicated for
postmenopausal women. Children: Not
ex-e-mes-tane indicated for use in this pt population.
(Aromasin) Elderly: No age-related precautions noted.
Do not confuse Aromasin with
Arimidex, or exemestane with INTERACTIONS
estramustine. DRUG: CYP3A4 inducers (e.g., PHE-
Nobarbital, rifAMPin) may decrease
uCLASSIFICATION concentration/effect. Estrogen deriva-
PHARMACOTHERAPEUTIC: Aromatase tives may decrease therapeutic effect.
inhibitor. CLINICAL: Antineoplastic. HERBAL: St. John’s wort may decrease
concentration. FOOD: None known. LAB
VALUES: May increase serum alkaline
USES phosphatase, ALT, AST.
Treatment of advanced breast cancer in
postmenopausal women whose disease AVAILABILITY (Rx)
has progressed following tamoxifen Tablets: 25 mg.
therapy. Adjuvant treatment of postmeno-
pausal women with estrogen receptor– ADMINISTRATION/HANDLING
positive early breast cancer after 2–3 yrs PO
of tamoxifen therapy for completion of • Give after meals.
5 consecutive yrs of adjuvant hormonal
therapy. OFF-LABEL: Reduces risk of inva- INDICATIONS/ROUTES/DOSAGE
sive breast cancer in postmenopausal Breast Cancer (Early)
women; treatment of endometrial cancer, PO: POSTMENOPAUSAL WOMEN: 25 mg
uterine sarcoma. once daily after a meal (following 2–3 yrs
tamoxifen therapy) for total duration of 5
PRECAUTIONS yrs of endocrine therapy (in absence of
Contraindications: Hypersensitivity to recurrence or contralateral breast cancer).
exemestane. Cautions: Not indicatedfor
use in premenopausal women. Concomi- Breast Cancer (Advanced)
tant use of estrogen-containing agents, PO: POSTMENOPAUSAL WOMEN: 25
strong CYP3A4 inducers. mg once daily after a meal. 50 mg/day
when used concurrently with potent
ACTION CYP3A4 inducers (e.g., rifAMPin, phenyt-
Inactivates aromatase, the principal oin). Continue until tumor progression.
enzyme that converts androgens to Dosage in Renal/Hepatic Impairment
estrogens in both premenopausal and No dose adjustment.
postmenopausal women, lowering cir-
culating estrogen level. Therapeutic SIDE EFFECTS
Effect: Inhibits growth of breast cancers Frequent (22%–10%): Fatigue, nausea,
stimulated by estrogens. depression, hot flashes, pain, insomnia,

underlined – top prescribed drug


exenatide 469
anxiety, dyspnea. Occasional (8%– PRECAUTIONS
5%): Headache, dizziness, vomiting, periph- Contraindications: Hypersensitivity to
eral edema, abdominal pain, anorexia, exenatide. Bydureon only: History of med-
flu-like symptoms, diaphoresis, constipa- ullary thyroid carcinoma. Pts with mul-
tion, hypertension. Rare (4%): Diarrhea. tiple endocrine neoplasia syndrome type 2
(MEN2). Cautions: Diabetic ketoacidosis,
ADVERSE EFFECTS/TOXIC
type 1 diabetes mellitus. Pts with renal
REACTIONS E
transplantation or moderate renal impair-
MI has been reported. ment. Not recommended in severe renal
impairment, severe GI disease, pancreatitis.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT ACTION
Question history of cardiac disease. Re- Stimulates release of insulin from beta
ceive full medication history and screen cells of pancreas, mimics enhancement of
for interactions. Offer emotional support. glucose-dependent insulin secretion, sup-
presses elevated glucagon secretion, slows
INTERVENTION/EVALUATION gastric emptying (central action increases
Monitor for onset of depression. Assess sleep satiety). Therapeutic Effect: Improves
pattern. Monitor for and assist with ambula- glycemic control by increasing postmeal
tion if dizziness occurs. Assess for headache. insulin secretion, decreasing postmeal
Offer antiemetic for nausea/vomiting. glucagon levels, delaying gastric emptying,
and increasing satiety.
PATIENT/FAMILY TEACHING
• Report if nausea, hot flashes become PHARMACOKINETICS
unmanageable. • Avoid tasks that re- Minimal systemic metabolism. Elimi-
quire alertness, motor skills until response nated by glomerular filtration with subse-
to drug is established. • Best taken after quent proteolytic degradation. Half-life:
meals and at same time each day. 2.4 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if dis-
tributed in breast milk. Children: Safety
and efficacy not established. Elderly: No
exenatide age-related precautions noted.

ex-en-a-tide
INTERACTIONS
(Bydureon, Bydureon BCise, Byetta, DRUG: May decrease concentration/
5 mcg Pen, 10 mcg Pen) effect of oral contraceptives. May
j BLACK BOX ALERT j(Bydu- increase hypoglycemic effect of insu-
reon): Risk of thyroid C-cell tumors. lin, sulfonylureas (e.g., glyburide).
HERBAL: None significant. FOOD: None
uCLASSIFICATION known. LAB VALUES: None known.
PHARMACOTHERAPEUTIC: Gluca-
gon-like peptide-1 (GLP-1) receptor AVAILABILITY (Rx)
agonist. CLINICAL: Antidiabetic. Injection, Solution (Prefilled Pen):
(Byetta): 10 mcg/0.04 mL (2.4 mL); 5
mcg/0.02 mL (1.2 mL). Injection, Sus-
USES pension: (Bydureon): 2 mg. Injection Pre-
Adjunct to diet, exercise to improve glycemic filled Single-Dose Auto-injector: (Bydureon
control in pts with type 2 diabetes mellitus. BCise): 2 mg in 0.85 ml vehicle.

Canadian trade name Non-Crushable Drug High Alert drug


470 ezetimibe

ADMINISTRATION/HANDLING NURSING CONSIDERATIONS


SQ
• May be given in thigh, abdomen, up- BASELINE ASSESSMENT
per arm. • Rotation of injection sites is Check serum glucose before administra-
essential; maintain careful injection site tion. Discuss lifestyle to determine extent
record. • Give within 60 min before of learning, emotional needs. Ensure fol-
morning and evening meals. Give suspen- low-up instruction if pt or family does not
E sion immediately after powder is sus- thoroughly understand diabetes manage-
pended. ment, glucose-testing technique. At least
Storage • Refrigerate prefilled pens. 1 mo should elapse to assess response to
• Discard if freezing occurs. • May be drug before new dose adjustment is made.
stored at room temperature after first INTERVENTION/EVALUATION
use. • Discard pen 30 days after initial
Monitor serum glucose, food intake,
use. • (Bydureon BCise): Remove
renal function. Assess for hypoglycemia
from refrigerator 15 min prior to mixing.
(cool wet skin, tremors, dizziness, anxi-
To mix, shake vigorously for at least 15 sec.
ety, headache, tachycardia, numbness in
INDICATIONS/ROUTE/DOSAGE mouth, hunger, diplopia), hyperglycemia
(polyuria, polyphagia, polydipsia, nausea,
Diabetes Mellitus
vomiting, dim vision, fatigue, deep rapid
SQ: ADULTS, ELDERLY: (Byetta) 5 mcg
breathing). Be alert to conditions that al-
per dose given twice daily within the
ter glucose requirements (fever, increased
60-min period before the morning and
activity or stress, surgical procedure).
evening meals. Dose may be increased to
10 mcg twice daily after 1 mo of therapy. PATIENT/FAMILY TEACHING
(Bydureon): 2 mg once q7days any time • Diabetes mellitus requires lifelong con-
of day, with or without meals. trol. • Prescribed diet and exercise are
principal parts of treatment. Do not skip,
Dosage in Renal Impairment
delay meals. • Continue to adhere to di-
Mild impairment: No dose adjustment.
etary instructions, regular exercise program,
Moderate impairment: Use caution.
regular testing of serum glucose. • When
Severe impairment: CrCl less than 30
taking combination therapy with a sulfonyl-
mL/min or ESRD: Not recommended. urea, have source of glucose available to
Dosage in Hepatic Impairment treat symptoms of hypoglycemia. • Report
No dose adjustment. any unexplained severe abdominal pain with
or without nausea or vomiting.
SIDE EFFECTS
(Byetta): Frequent (44%): Nausea. Occa-
sional (13%–6%): Diarrhea, vomiting,
ezetimibe
dizziness, anxiety, dyspepsia. Rare (less e-zet-i-mib
than 6%): Weakness. (Bydureon): 5% or
(Ezetrol , Zetia)
greater: Nausea, diarrhea, headache,
Do not confuse Zetia with
constipation, vomiting, dyspepsia, injec- Zebeta or Zestril.
tion site pruritus or nodule.
FIXED-COMBINATION(S)
ADVERSE EFFECTS/TOXIC
REACTIONS Liptruzet: ezetimibe/atorvastatin
(statin): 10 mg/10 mg, 10 mg/20 mg,
With concurrent sulfonylurea, hypoglyce- 10 mg/40 mg, 10 mg/80 mg. Vyto-
mia occurs in 36% when given a 10-mcg rin: ezetimibe/simvastatin (statin):
dose of exenatide, 16% when given a 10 mg/10 mg, 10 mg/20 mg, 10
5-mcg dose. May cause acute pancreatitis. mg/40 mg, 10 mg/80 mg.
underlined – top prescribed drug
ezetimibe 471
uCLASSIFICATION or younger. Elderly: Age-related mild
PHARMACOTHERAPEUTIC: Antihy- hepatic impairment may require dosage
perlipidemic. CLINICAL: Anticholes- adjustment.
terol agent.
INTERACTIONS
DRUG: Bile acid sequestrants (e.g.,
USES cholestyramine) may decrease absorp-
Adjunct to diet for treatment of primary tion/effect. May increase concentration/ E
hypercholesterolemia (monotherapy or effect of cycloSPORINE. Fenofibrate
in combination with HMG-CoA reductase and derivatives, gemfibrozil may
inhibitors [statins]), homozygous sitos- increase adverse effects. HERBAL: None
terolemia, homozygous familial hypercho- significant. FOOD: None known. LAB
lesterolemia (combined with atorvastatin VALUES: May increase serum alkaline
or simvastatin). Mixed hyperlipidemia (in phosphatase, bilirubin, ALT, AST.
combination with fenofibrate).
AVAILABILITY (Rx)
PRECAUTIONS Tablets: 10 mg.
Contraindications: Hypersensitivity to
ezetimibe. Concurrent use of an HMG-CoA ADMINISTRATION/HANDLING
reductase inhibitor (atorvastatin, fluvastatin, • Give without regard to food. • May
lovastatin, pravastatin, simvastatin) in pts give at same time as statins. Give at least
with active hepatic disease or unexplained 2 hrs before or 4 hrs after bile acid se-
persistent elevations in serum transami- questrants.
nase; pregnancy and breastfeeding (when
used with a statin). Cautions: Severe renal INDICATIONS/ROUTES/DOSAGE
or mild hepatic impairment. Not recom- Hypercholesterolemia
mended in those with moderate or severe PO: ADULTS, ELDERLY, CHILDREN 10 YRS
hepatic impairment. AND OLDER: Initially, 10 mg once daily,
given with or without food. If pt is also
ACTION receiving a bile acid sequestrant, give
Inhibits cholesterol absorption in brush ezetimibe at least 2 hrs before or at least
border of small intestine, leading to 4 hrs after bile acid sequestrant.
decrease in delivery of intestinal choles-
Dosage in Renal Impairment
terol to liver. Reduces hepatic cholesterol
stores and increases clearance of cho- No dose adjustment.
lesterol from the blood. Therapeutic Dosage in Hepatic Impairment
Effect: Reduces total serum cholesterol, Mild impairment: No dose adjustment.
LDL, triglycerides; increases HDL. Moderate to severe impairment: Not
PHARMACOKINETICS recommended.
Well absorbed following PO administra- SIDE EFFECTS
tion. Protein binding: greater than 90%. Occasional (4%–3%): Back pain, diar-
Metabolized in small intestine and liver. rhea, arthralgia, sinusitis, abdominal
Excreted in feces (78%), urine (11%). pain. Rare (2%): Cough, pharyngitis,
Half-life: 22 hrs. fatigue, depression.
LIFESPAN CONSIDERATIONS ADVERSE EFFECTS/TOXIC
Pregnancy/Lactation: Unknown if REACTIONS
drug crosses placenta or is distributed Hepatitis, hypersensitivity reaction,
in breast milk. Children: Safety and myopathy, rhabdomyolysis occur rarely.
efficacy not established in pts 10 yrs
Canadian trade name Non-Crushable Drug High Alert drug
472 ezetimibe
INTERVENTION/EVALUATION
NURSING CONSIDERATIONS
Monitor daily pattern of bowel activity,
BASELINE ASSESSMENT stool consistency. Question pt for signs/
Obtain diet history, esp. fat consumption. symptoms of back pain, abdominal dis-
Obtain serum cholesterol, triglycerides, turbances. Monitor serum cholesterol,
hepatic function tests, blood counts dur- triglycerides for therapeutic response.
ing initial therapy and periodically during
E PATIENT/FAMILY TEACHING
treatment. Treatment should be discon-
tinued if hepatic enzyme levels persist • Periodic laboratory tests are essential
more than 3 times normal limit. Receive part of therapy. • Do not stop medica-
full medication history and screen for tion without consulting physician. • Re-
interactions. Question history of hepatic/ port muscular or bone pain. • May
renal impairment. take at same time as statins. Take at least
2 hrs before or 4 hrs after cholestyr-
amine, colestipol, colesevelam.

underlined – top prescribed drug


famciclovir 473
LIFESPAN CONSIDERATIONS
famciclovir Pregnancy/Lactation: Unknown if ex­
creted in breast milk. Children: Safety
fam-sye-klo-veer and efficacy not established. El-
(Apo-Famciclovir , Famvir ) derly: Age-related renal impairment
Do not confuse famciclovir may require dosage adjustment.
with acyclovir, ganciclovir, or
valGANciclovir; or Famvir with INTERACTIONS
Femara. DRUG: None significant. HERBAL: None
significant. FOOD: None known. LAB F
uCLASSIFICATION
VALUES: May increase serum ALT, AST,
PHARMACOTHERAPEUTIC: Synthetic amylase, bilirubin, lipase. May decrease
nucleoside. CLINICAL: Antiviral. neutrophils, platelets.

AVAILABILITY (Rx)
USES
Tablets: 125 mg, 250 mg, 500 mg.
Treatment of acute herpes zoster (shingles)
in immunocompetent pts, treatment and
suppression of recurrent genital herpes in ADMINISTRATION/HANDLING
immunocompetent pts, treatment of recur- PO
rent mucocutaneous herpes simplex in • Give without regard to food. • Give
HIV-infected pts. Treatment of recurrent with food to decrease GI distress.
herpes labialis (cold sores) in immuno-
competent pts. INDICATIONS/ROUTES/
DOSAGE
PRECAUTIONS Herpes Zoster (Shingles)
Contraindications: Hypersensitivity to fam- PO: ADULTS: 500 mg q8h for 7 days.
ciclovir, penciclovir. Cautions: Renal im- Begin as soon as possible after diag-
pairment. Avoid use in galactose intoler- nosis and within 72 hrs of rash onset.
ance, severe lactose deficiency, or (HIV pts): 500 mg 3 times/day for 7–10
glucose-galactose malabsorption syn- days.
dromes.
ACTION Genital Herpes Simplex (Initial)
Inhibits HSV-2 polymerase, inhibiting PO: ADULTS: 250 mg 3 times/day for
herpes viral DNA synthesis and replica- 7–10 days. (HIV pts): 500 mg twice daily
tion. Therapeutic Effect: Suppresses for 5-10 days.
replication of herpes simplex virus, var-
icella-zoster virus. Shortens healing time Genital Herpes Simplex (Recurrence)
of herpes zoster lesions. Reduces symp- PO: ADULTS: 1,000 mg twice daily for
tom severity of genital herpes. 1 day; or 125 mg 2 times/day for 5
days; or 500 mg once, then 250 mg 2
PHARMACOKINETICS times/day for 2 days. (HIV pts): 500 mg
Rapidly absorbed. Protein binding: 20%– twice daily for 5-10 days.
25%. Rapidly metabolized to penciclovir
by enzymes in GI tract, liver, plasma. Genital Herpes Simplex (Suppression)
Excreted unchanged in urine. Removed PO: ADULTS: 250 mg twice daily for up
by hemodialysis. Half-life: 2–3 hrs to 1 yr. (HIV pts): 500 mg twice daily con-
(increased in severe renal failure). tinued indefinitely.

Canadian trade name Non-Crushable Drug High Alert drug


474 famotidine
Herpes Labialis (Cold Sores) Dosage in Renal Impairment
PO: ADULTS, ELDERLY: (Immunocompetent): Dosage and frequency are modified
1,500 mg as a single dose. Initiate at based on creatinine clearance and dis-
first sign or symptoms. (HIV pts): 500 mg ease process.
2 times/day for 5–10 days.

Recurrent Recurrent Recurrent


Genital Herpes Labialis Orolabial or
Herpes Recurrent Treatment Genital
F Creatinine Herpes (single-day Genital Herpes (single-day Herpes
Clearance Zoster regimen) (suppression) regimen) in HIV Pts
40–59 mL/min 500 mg q12h 500 mg q12h — 750 mg —
20–39 mL/min 500 mg q24h 500 mg 125 mg q12h 500 mg 500 mg q24h
Less than 250 mg q24h 250 mg 125 mg q24h 250 mg 250 mg q24h
20 mL/min
Hemodialysis 250 mg after 250 mg after 125 mg after 250 mg after 250 mg after
each he­ each he­ each hemo­ each hemo­ each hemo­
modialysis modialysis dialysis dialysis ses­ dialysis
session session session sion session

Dosage in Hemodialysis Pts INTERVENTION/EVALUATION


Herpes zoster: 250 mg after each dial- Evaluate cutaneous lesions. Be alert to
ysis treatment. Genital herpes: 125 mg neurologic effects: headache, dizziness.
after each dialysis treatment. Provide analgesics, comfort measures.
Monitor renal function, hepatic enzymes,
Dosage in Hepatic Impairment
CBC.
No dose adjustment.
PATIENT/FAMILY TEACHING
SIDE EFFECTS • Drink adequate fluids. • Fingernails
Frequent (23%–12%): Headache, nausea. should be kept short, hands clean. • Do
Occa­sional (10%–2%): Dizziness, drowsi- not touch lesions with fingers to avoid
ness, paresthesia (esp. feet), diarrhea, vomit- spreading infection to new site. • Geni-
ing, constipation, decreased appetite, fatigue, tal herpes: Continue therapy for full
fever, pharyngitis, sinusitis, pruritus. Rare length of treatment. • Avoid contact with
(less than 2%): Insomnia, abdominal pain, lesions during duration of outbreak to
dyspepsia, flatulence, back pain, arthralgia. prevent cross-contamination. • Use con-
doms during sexual activity. • Report if
ADVERSE EFFECTS/TOXIC lesions recur or do not improve. • Slowly
REACTIONS go from lying to standing to avoid dizzi-
Urticaria, severe skin rash, hallucinations, ness. • Avoid tasks that require alert-
confusion (delirium, disorientation occur ness, motor skills until response to drug is
predominantly in elderly) has been reported. established.

NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Obtain baseline chemistry tests, esp. renal
famotidine
function. Question history of galactose fa-moe-ta-deen
intolerance, severe lactose deficiency, (Acid Reducer Maximum Strength,
glucose-galactose malabsorption, renal Apo-Famotidine , Pepcid,
impairment. Assess herpetic lesions. Ulcidine )

underlined – top prescribed drug


famotidine 475
Do not confuse famotidine with metabolized in liver. Primarily excreted
cimetidine, ranitidine, fluox- in urine. Not removed by hemodialysis.
etine, or furosemide. Half-life: 2.5–3.5 hrs (increased in renal
impairment).
FIXED-COMBINATION(S)
Duexis: famotidine/ibuprofen (an LIFESPAN CONSIDERATIONS
NSAID): 26.6 mg/800 mg. Pepcid Pregnancy/Lactation: Unknown if
Complete: famotidine/calcium chlo- drug crosses placenta or is distributed
ride/magnesium hydroxide (antacids): in breast milk. Children: No age-related
10 mg/800 mg/165 mg. precautions noted. Elderly: Confusion F
more likely to occur, esp. in pts with
uCLASSIFICATION renal/hepatic impairment.
PHARMACOTHERAPEUTIC: H2 recep-
tor antagonist. CLINICAL: Antiulcer, INTERACTIONS
gastric acid secretion inhibitor. DRUG: May decrease absorption of ata-
zanavir, cefuroxime, itraconazole,
ketoconazole. May decrease concen-
USES tration/effect of neratinib, pazopanib.
Short-term treatment of active duodenal May increase concentration/effect of
ulcer. Prevention, maintenance of duode- risedronate. HERBAL: None significant.
nal ulcer recurrence. Treatment of active FOOD: None known. LAB VALUES: Inter-
benign gastric ulcer, pathologic GI hyper- feres with skin tests using allergen extracts.
secretory conditions. Short-term treatment May increase serum alkaline phosphatase,
of gastroesophageal reflux disease (GERD). ALT, AST. May decrease platelet count.
OTC formulation for relief of heartburn,
acid indigestion, sour stomach. OFF-LABEL: AVAILABILITY (Rx)
H. pylori eradication, risk reduction of Infusion, Premix: 20 mg in 50 mL 0.9%
duodenal ulcer recurrence (part of multi- NaCl. Injection, Solution: 10 mg/mL (2-mL
drug regimen), stress ulcer prophylaxis in vial). Powder for Oral Suspension: 40
critically ill pts, relief of gastritis. mg/5 mL. Tablets: 10 mg, 20 mg, 40 mg.
PRECAUTIONS
ADMINISTRATION/HANDLING
Contraindications: Hypersensitivity to
famotidine, other H2 antagonists. OTC: IV
Avoid use in pts with dysphagia, odynopha- Reconstitution • For IV push, dilute
gia, hematemesis, melena, hematochezia, 20 mg with 5–10 mL 0.9% NaCl. • For
renal impairment. Cautions: Renal/hepatic intermittent IV infusion (piggyback), di-
impairment, elderly, thrombocytopenia. lute with 50–100 mL D5W, or 0.9% NaCl.
ACTION Rate of administration • Give IV
push over at least 2 min. • Infuse pig-
Inhibits histamine action of H2 receptors of gyback over 15–30 min.
parietal cells. Therapeutic Effect: Inhib- Storage • Refrigerate unused vials.
its gastric acid secretion (fasting, nocturnal, • IV solution appears clear, colorless.
or stimulated by food, caffeine, insulin). • After dilution, IV solution is stable for
PHARMACOKINETICS 48 hrs if refrigerated.
Route Onset Peak Duration
PO
PO 1 hr 1–4 hrs 10–12 hrs
IV 0.5 hr 0.5–3 hrs 10–12 hrs • Store tablets, suspension at room tem-
perature. • Following reconstitution,
Rapidly, incompletely absorbed from GI oral suspension is stable for 30 days at
tract. Protein binding: 15%–20%. Partially room temperature. • Give without re-
Canadian trade name Non-Crushable Drug High Alert drug
476 famotidine
gard to meals. • Shake suspension well 20–40 mg twice daily for up to
(Tablets):
before use. 12 wks. CHILDREN (Suspension): 0.5 mg/
kg twice daily. Maximum: 40 mg twice
IV INCOMPATIBILITIES daily.
Amphotericin B complex (Abelcet, AmBi-
some, Amphotec), piperacillin/tazobac- Hypersecretory Conditions
tam (Zosyn). PO: ADULTS, ELDERLY, CHILDREN 17 YRS
AND OLDER: Initially, 20 mg q6h. May
IV COMPATIBILITIES increase up to 160 mg q6h.
F Calcium gluconate, dexamethasone
(Decadron), dexmedetomidine (Prece- Acid Indigestion, Heartburn (OTC Use)
dex), DOBUTamine (Dobutrex), DOPamine PO: ADULTS, ELDERLY, CHILDREN 12 YRS
(Intropin), DOXOrubicin (Adriamycin), AND OLDER: 10–20 mg q12h. May take
furosemide (Lasix), heparin, HYDROmor- 15–60 min before eating. Maximum: 2
phone (Dilaudid), insulin (regular), lido- doses/day.
caine, LORazepam (Ativan), magnesium
Usual Parenteral Dosage
sulfate, midazolam (Versed), morphine,
IV: ADULTS, ELDERLY, CHILDREN OLDER
nitroglycerin, norepinephrine (Levophed),
THAN 12 YRS: 20 mg q12h. CHILDREN
ondansetron (Zofran), potassium chloride,
1–12 YRS: 0.25–0.5 mg/kg q12h. Maxi-
potassium phosphate, propofol (Diprivan).
mum: 40 mg/day.
INDICATIONS/ROUTES/DOSAGE Dosage in Renal Impairment
Duodenal Ulcer Creatinine
PO: ADULTS, ELDERLY: ADOLESCENTS, CHIL- Clearance Dosage
DREN WEIGHING MORE THAN 40 KG (Tab- Less than 50% normal dose or increase
lets): Acute therapy: 40 mg/day at bedtime 50 mL/min dosing interval to 48 hrs
or 20 mg twice daily for 4–8 wks. Mainte-
nance: 20 mg/day at bedtime. CHILDREN Dosage in Hepatic Impairment
(Suspension): 0.5 mg/kg/day at bedtime or No dose adjustment.
divided twice daily. Maximum: 40 mg/day.
SIDE EFFECTS
Gastric Ulcer Occasional (5%): Headache. Rare (2% or
PO: ADULTS, ELDERLY: ADOLESCENTS, CHIL- less): Confusion, constipation, diarrhea,
DREN WEIGHING MORE THAN 40 KG (Tablets, dizziness.
Acute therapy): 40 mg/day at bedtime. for
up to 8 wks. CHILDREN (Suspension): 0.5 mg/ ADVERSE EFFECTS/TOXIC
kg/day at bedtime or divided twice daily. REACTIONS
Maximum: 40 mg/day. Agranulocytosis, pancytopenia, thrombo-
cytopenia occur rarely.
Gastroesophageal Reflux Disease (GERD)
PO: ADULTS, ELDERLY: ADOLESCENTS, CHIL- NURSING CONSIDERATIONS
DREN WEIGHING MORE THAN 40 KG (Tablets):
BASELINE ASSESSMENT
20 mg twice daily for 6 wks. CHILDREN
1–16 YRS: 1 mg/kg/day in 2 divided doses. Assess epigastric/abdominal pain. Verify
Maximum: 40 mg 2 times/day. CHILDREN platelet count in critically ill pts.
3 MOS–11 MOS: 0.5 mg/kg/dose twice INTERVENTION/EVALUATION
daily. CHILDREN YOUNGER THAN 3 MOS, NEO- Monitor daily pattern of bowel activity, stool
NATES: 0.5 mg/kg/dose once daily.
consistency. Monitor for headache. Assess
Esophagitis for confusion in elderly. Consider interrupt-
PO: ADULTS, ELDERLY, ADOLESCENTS, ing treatment in pts who develop thrombo-
CHILDREN WEIGHING 40 KG OR MORE: cytopenia.

underlined – top prescribed drug


febuxostat 477

PATIENT/FAMILY TEACHING milk. Children: Safety and efficacy not


• May take without regard to food, ant- established. Elderly: No age-related pre-
acids. • Report headache. • Avoid cautions noted.
excessive amounts of coffee, aspirin.
INTERACTIONS
• Report persistent symptoms of heart-
burn, acid indigestion, sour stomach. DRUG: May increase concentration,
toxicity of azaTHIOprine, mercapto-
purine, theophylline. HERBAL: None
significant. FOOD: None known. LAB
febuxostat VALUES: May increase serum alkaline
phosphatase, ALT, AST, LDH, amylase,
F

fe-bux-oh-stat sodium, potassium, cholesterol, triglyc-


(Uloric) erides, BUN, creatinine. May decrease
Do not confuse febuxostat with platelets, Hgb, Hct, neutrophils. May pro-
panobinostat or Femstat. long prothrombin time.

uCLASSIFICATION AVAILABILITY (Rx)


PHARMACOTHERAPEUTIC: Xanthine Tablets: 40 mg, 80 mg.
oxidase inhibitor. CLINICAL: Antigout
ADMINISTRATION/HANDLING
agent.
PO
• Give without regard to food or antac-
USES ids.
Chronic management of hyperuricemia in
pts with gout. Not recommended for treat- INDICATIONS/ROUTES/DOSAGE
ment of asymptomatic hyperuricemia. b ALERT c Recommended concomi-
tant NSAID or colchicine with initiation of
PRECAUTIONS therapy and continue for up to 6 mos to
Contraindications: Hypersensitivity to prevent exacerbations of gout.
febuxostat. Concomitant use with azaTHIO-
Hyperuricemia
prine, mercaptopurine. Cautions: Severe
renal/hepatic impairment, history of heart PO: ADULTS, ELDERLY: Initially, 40 mg
disease or stroke. Hypersensitivity to allo- once daily. If pt does not achieve serum
purinol. Pts at risk for urate formation. uric acid level less than 6 mg/dL after 2
wks with 40 mg, may give 80 mg once
ACTION daily. Maximum: 120 mg/day.
Decreases uric acid production by selec- Dosage in Renal/Hepatic Impairment
tively inhibiting the enzyme xanthine oxi- Mild to moderate impairment: No
dase. Therapeutic Effect: Reduces uric dose adjustment. Severe impairment:
acid concentrations in serum and urine. Use caution.
PHARMACOKINETICS SIDE EFFECTS
Well absorbed from GI tract. Widely dis- Rare (1%): Nausea, arthralgia, rash,
tributed. Protein binding: 99%. Metabo- dizziness.
lized in liver. Excreted in urine (49%),
feces (45%). Removed by hemodialysis. ADVERSE EFFECTS/TOXIC
Half-life: 5–8 hrs. REACTIONS
LIFESPAN CONSIDERATIONS Hepatic function abnormalities occur in
6% of pts. May increase risk of thrombo-
Pregnancy/Lactation: Unknown if drug embolic events including CVA, MI.
crosses placenta or is distributed in breast
Canadian trade name Non-Crushable Drug High Alert drug
478 felodipine

PRECAUTIONS
NURSING CONSIDERATIONS
Contraindications: Hypersensitivity to
BASELINE ASSESSMENT felodipine or other calcium channel
Assess baseline renal function, LFT; con- blocker. Cautions: Severe left ventricu-
comitant use with azaTHIOprine, mercap- lar dysfunction, HF, hepatic impairment,
topurine, theophylline (contraindicated). hypertrophic cardiomyopathy with out-
flow tract obstruction, peripheral edema,
INTERVENTION/EVALUATION severe aortic stenosis, elderly. Concomi-
Discontinue medication immediately if tant CYP3A4 inhibitors.
F rash appears. Encourage high fluid intake
(3,000 mL/day). Monitor I&O (output ACTION
should be at least 2,000 mL/day). Moni- Inhibits calcium movement across car-
tor CBC, serum uric acid, renal function, diac, vascular smooth muscle cell mem-
LFT. Assess urine for cloudiness, unusual branes. Therapeutic Effect: Relaxes
color, odor. Assess for therapeutic re- coronary vascular smooth muscle and
sponse (reduced joint tenderness, swell- causes vasodilation. Increases myocar-
ing, redness, limitation of motion). Moni- dial oxygen delivery. Reduces B/P.
tor for symptoms of CVA, MI.
PHARMACOKINETICS
PATIENT/FAMILY TEACHING
Route Onset Peak Duration
• Encourage drinking 8–10 (8-oz)
PO 2–5 hrs N/A 24 hrs
glasses of fluid daily while taking medica-
tion. • Report rash, chest pain, shortness Rapidly, completely absorbed from GI
of breath, symptoms suggestive of tract. Protein binding: greater than 99%.
stroke. • Gout attacks may occur for sev- Metabolized in liver. Primarily excreted
eral months after starting treatment (medi- in urine. Not removed by hemodialysis.
cation is not a pain reliever). • Continue Half-life: 11–16 hrs.
taking even if gout attack occurs.
LIFESPAN CONSIDERATIONS
felodipine Pregnancy/Lactation: Unknown if
drug crosses placenta or is distributed
in breast milk. Children: Safety and
fe-loe-di-peen
efficacy not established. Elderly: May
(Plendil )
experience greater hypotensive response.
Do not confuse Plendil with Isor-
Constipation may be more problematic.
dil, Pletal, PriLOSEC, or Prinivil.
FIXED-COMBINATION(S) INTERACTIONS
DRUG: Strong CYP3A4 inhibitors
Lexxel: felodipine/enalapril (ACE in-
(e.g., clarithromycin, ketoconazole,
hibitor): 2.5 mg/5 mg, 5 mg/5 mg.
ritonavir), cimetidine may increase
uCLASSIFICATION concentration/effect. Strong CYP3A4
inducers (e.g., carBAMazepine, phe-
PHARMACOTHERAPEUTIC: Calcium
nytoin, rifAMPin) may decrease concen-
channel blocker (dihydropyridine).
tration/effect. May increase concentration/
CLINICAL: Antihypertensive.
effect of phenytoin. HERBAL: St. John’s
wort may decrease concentration/effect.
USES Herbals with hypotensive properties
Management of hypertension. May be (e.g., garlic, ginger, gingko biloba)
used alone or with other antihyperten- may increase effect. Herbals with hyper-
sives. OFF-LABEL: Management of pediat- tensive properties (e.g., yohimbe)
ric hypertension. may decrease effect. FOOD: Grapefruit
underlined – top prescribed drug
fenofibrate 479

products may increase absorption, con- physician). Question history of HF, he-
centration. LAB VALUES: None significant. patic impairment, valvular disease.
AVAILABILITY (Rx) INTERVENTION/EVALUATION

Tablets: (Extended-Release): 2.5 mg, Assist with ambulation if dizziness oc-


5 mg, 10 mg. curs. Assess for peripheral edema. Moni-
tor pulse rate for bradycardia. Assess
ADMINISTRATION/HANDLING skin for flushing. Monitor hepatic func-
tion. Question for headache, asthenia.
PO
• Give with or without food. • Do not PATIENT/FAMILY TEACHING
F
break, crush, dissolve, or divide ex- • Do not abruptly discontinue medica-
tended-release tablets. Swallow whole. tion. • Compliance with therapy regimen
is essential to control hypertension. • To
INDICATIONS/ROUTES/DOSAGE avoid hypotensive effect, go from lying to
Hypertension standing slowly. • Avoid tasks that re-
PO: ADULTS: Initially, 2.5–5 mg once daily. quire alertness, motor skills until response
Increase by 5 mg at 1–2 wk intervals. Usual to drug is established. • Report palpita-
dose: 2.5–10 mg once daily. ELDERLY: Ini- tions, shortness of breath, pronounced
tially, 2.5 mg/day. Adjust dosage at no less dizziness, nausea. • Swallow tablet
than 2-wk intervals. Usual dose: 2.5–10 mg whole; do not chew, crush, dissolve, or
once daily. CHILDREN 6 YRS AND OLDER: Ini- divide. • Avoid grapefruit products, al-
tially, 2.5 mg once daily. May increase at cohol. • Report exacerbation of angina.
2-wk intervals. Maximum: 10 mg/day.
Dosage in Renal Impairment
No dose adjustment. fenofibrate
Dosage in Hepatic Impairment
Initially, 2.5 mg once daily. Titrate car­efully. fen-o-fye-brate
(Antara, Fenoglide, Fibricor,
SIDE EFFECTS Lipofen, Lipidil EZ , Tricor,
Frequent (22%–18%): Headache, periph- Triglide, Trilipix)
eral edema. Occasional (6%–4%): Flush- Do not confuse Tricor with
ing, respiratory infection, dizziness, Fibricor or Tracleer.
light-headedness, asthenia. Rare (less than uCLASSIFICATION
3%): Angina, gingival hyperplasia, paresthe-
sia, abdominal discomfort, anxiety, muscle PHARMACOTHERAPEUTIC: Fibric
cramping, cough, diarrhea, constipation. acid derivative. CLINICAL: Antihy-
perlipidemic.
ADVERSE EFFECTS/TOXIC
REACTIONS USES
Overdose produces nausea, drowsiness,
Adjunct to diet for reduction of low-
confusion, slurred speech, hypotension,
density lipoprotein cholesterol (LDL-C),
bradycardia.
total cholesterol, triglycerides (types IV
NURSING CONSIDERATIONS and V hyperlipidemia), apo-lipoprotein
B, and to increase high-density lipo-
BASELINE ASSESSMENT protein cholesterol (HDL-C) in pts with
Assess B/P, apical pulse immediately be- primary hypercholesterolemia, mixed
fore drug administration (if pulse is 60 dyslipidemia. Adjunctive therapy to diet
or less/min or systolic B/P is less than for treatment of severe hypertriglyceride-
90 mm Hg, withhold medication, contact mia (Fredrickson types IV and V).
Canadian trade name Non-Crushable Drug High Alert drug
480 fenofibrate

PRECAUTIONS AVAILABILITY (Rx)


Contraindications: Hypersensitivity to Capsules: 30 mg, 43 mg, 50 mg, 67
fenofibrate. Active hepatic disease, preex- mg, 90 mg, 130 mg, 134 mg, 150 mg,
isting gallbladder disease, severe renal/ 200 mg. Capsules, Delayed-Release: 45
hepatic dysfunction (including primary mg, 135 mg. Tablets: 35 mg, 40 mg,
biliary cirrhosis, unexplained persistent 48 mg, 54 mg, 105 mg, 120 mg,145 mg,
hepatic function abnormality), breast- 160 mg.
feeding. End-stage renal disease (ESRD).
Cautions: Anticoagulant therapy (e.g., war- ADMINISTRATION/HANDLING
F farin), history of hepatic disease, venous PO
thromboembolism, mild to moderate renal • Give Fenoglide, Lipofen, Lofibra
impairment, substantial alcohol consump- with meals. • Antara, Fibricor, Tricor,
tion, statin or colchicine therapy (increased Triglide, and Trilipix may be given
risk of myopathy, rhabdomyolysis), elderly. without regard to food. Antara, Feno-
ACTION glide, Lipofen: Swallow whole; do not
open (capsules), crush, dissolve,
Downregulates apoprotein C-III and or cut.
upregulates synthesis of apoprotein A-I,
fatty acid transport protein, and lipopro-
tein lipase, increasing VLDL catabolism. INDICATIONS/ROUTES/DOSAGE
Therapeutic Effect: Decreases triglycer- Hypertriglyceridemia
ides, VLDL levels, modestly increases HDL. PO: (Antara): ADULTS, ELDERLY: 30–90
mg/day. (Fenofibrate): ADULTS, ELDERLY:
PHARMACOKINETICS 43–130 mg/day. (Fenoglide): ADULTS,
Well absorbed from GI tract. Absorption ELDERLY: 40–120 mg/day with meals.
increased when given with food. Protein (Fibricor): ADULTS, ELDERLY: 35–105
binding: 99%. Metabolized in liver. Excreted mg/day. (Lipofen): ADULTS, ELDERLY:
in urine (60%), feces (25%). Not removed 50–150 mg/day with meals. (Lofibra):
by hemodialysis. Half-life: 10–35 hrs. ADULTS, ELDERLY: (micronized) 67–200
mg/day with meals; (tablets): 54-160 mg/
LIFESPAN CONSIDERATIONS day. (Tricor): ADULTS, ELDERLY: 48–145
Pregnancy/Lactation: Safety in preg- mg/day. (Triglide): ADULTS, ELDERLY: 160
nancy not established. Breastfeeding not mg/day. (Trilipix): ADULTS, ELDERLY: 45–
recommended. Children: Safety and 135 mg/day.
efficacy not established. Elderly: No
age-related precautions noted. Hypercholesterolemia, Mixed
Hyperlipidemia
INTERACTIONS PO: (Antara): ADULTS, ELDERLY: 90 mg/
DRUG: Potentiates effects of antico- day. (Fenofibrate): ADULTS, ELDERLY:
agulants (e.g., warfarin). Bile acid 130 mg/day. (Fenoglide): ADULTS,
sequestrants may impede absorption. ELDERLY: 120 mg/day with meals.
CycloSPORINE may increase concen- (Fibricor): ADULTS, ELDERLY: 105 mg/
tration, risk of nephrotoxicity. Colchi- day. (Lipofen): ADULTS, ELDERLY: 150
cine, HMG-CoA reductase inhibitors mg/day with meals. (Lofibra): ADULTS,
(statins) may increase risk of severe ELDERLY: (micronized) 200 mg/day with
myopathy, rhabdomyolysis, acute renal fail- meals; (tablets): 160 mg/day. (Tricor):
ure. HERBAL: None significant. FOOD: All ADULTS, ELDERLY: 145 mg/day. (Tri­
foods increase absorption. LAB VAL- glide): ADULTS, ELDERLY: 160 mg/day.
UES: May increase serum creatine kinase (Trilipix): ADULTS, ELDERLY: 135 mg/day.
(CK), ALT, AST. May decrease Hgb, Hct,
WBC; serum uric acid.
underlined – top prescribed drug
fentaNYL 481
Dosage in Renal Impairment PATIENT/FAMILY TEACHING
Monitor renal function before adjusting • Report severe diarrhea, constipation,
dose. Decrease dose or increase dosing nausea. • Report skin rash/irritation,
interval for pts with renal failure. insomnia, muscle pain, tremors, dizziness.
Initial Antara: Lofibra:
doses: 30 mg/day 67 mg/day
Fenoglide: Tricor:
40 mg/day
Lipofen:
48 mg/day
Triglide:
fentaNYL
50 mg/day 50 mg/day F
fen-ta-nil
(Abstral, Actiq, Fentora, Ionsys,
Dosage in Hepatic Impairment Lazanda, Sublimaze, Subsys)
Contraindicated. j BLACK BOX ALERT jPhysical
and psychological dependence may
SIDE EFFECTS occur with prolonged use. Must
Frequent (8%–4%): Pain, rash, headache, be alert to abuse, misuse, or diver­
asthenia, fatigue, flu-like symptoms, dyspep- sion. May cause life-threatening
hypoventilation, respiratory depres­
sia, nausea/vomiting, rhinitis. Occasional sion, or death. Use with strong or
(3%–2%): Diarrhea, abdominal pain, con- moderate CYP3A4 inhibitors may
stipation, flatulence, arthralgia, decreased result in potentially fatal respiratory
libido, dizziness, pruritus. Rare (less than depression. Buccal: Tablet and
2%): Increased appetite, insomnia, polyuria, lozenge contain enough medication
to potentially be fatal to children.
cough, blurred vision, eye floaters, earache. Transdermal patch: Serious or
life-threatening hypoventilation has
ADVERSE EFFECTS/TOXIC occurred. Limit use to children 2 yrs
REACTIONS of age and older. Exposure to direct
May increase cholesterol excretion into heat source increases drug release,
resulting in overdose/death.
bile, leading to cholelithiasis. Pancreati-
Do not confuse fentaNYL with
tis, hepatitis, thrombocytopenia, agranu-
alfentanil or SUFentanil.
locytosis occur rarely.
uCLASSIFICATION
NURSING CONSIDERATIONS
PHARMACOTHERAPEUTIC: Opioid,
BASELINE ASSESSMENT narcotic agonist (Schedule II).
Obtain diet history, esp. fat consumption. CLINICAL: Analgesic.
Obtain serum cholesterol, triglycerides,
LFT, CBC during initial therapy and periodi-
cally during treatment. Treatment should be USES
discontinued if hepatic enzyme levels per- Injection: (FentaNYL): Pain relief,
sist greater than 3 times normal limit. Ques- preop medication; adjunct to general or
tion medical history as listed in Precautions. regional anesthesia. Abstral: Treatment
of breakthrough pain in cancer pts 18
INTERVENTION/EVALUATION yrs of age and older. Actiq: Treatment
For pts on concurrent therapy with HMG- of breakthrough pain in chronic can-
CoA reductase inhibitors, monitor for cer or AIDS-related pain. Duragesic:
complaints of myopathy (muscle pain, Management of chronic pain (transder-
weakness). Monitor serum creatine ki- mal). Fentora: Breakthrough pain in
nase (CK). Monitor serum cholesterol, pts on chronic opioids. Ionsys: Short-
triglyceride for therapeutic response. term management of acute postoperative

Canadian trade name Non-Crushable Drug High Alert drug


482 fentaNYL
pain in adults. Lazanda: Management of liver. Primarily excreted by biliary system.
breakthrough pain in cancer. Onsolis: Half-life: 2–4 hrs IV; 17 hrs transder-
Breakthrough pain in pts with cancer mal; 6.6 hrs transmucosal.
currently receiving opioids and tolerant
to opioid therapy. Subsys: Treatment of LIFESPAN CONSIDERATIONS
breakthrough cancer pain. Pregnancy/Lactation: Readily crosses
placenta. Unknown if distributed in breast
PRECAUTIONS milk. May prolong labor if administered in
Contraindications: Hypersensitivity to latent phase of first stage of labor or before
F fen­­taNYL. Transdermal device (addi- cervical dilation of 4–5 cm has occurred.
tional): Significant respiratory depres- Respiratory depression may occur in
sion, acute/severe bronchial asthma, neonate if mother received opiates dur-
paralytic ileus, GI obstruction. Trans- ing labor. Children: Neonates more sus-
dermal patch (additional): Signifi- ceptible to respiratory depressant effects.
cant respiratory depression, acute/severe Patch: Safety and efficacy not established
bronchial asthma, paralytic ileus, short- in pts younger than 12 yrs. Elderly: May
term therapy for acute or postoperative be more susceptible to respiratory depres-
pain, pts who are not opioid tolerant. sant effects. Age-related renal impairment
Transmucosal buccal, buccal films, may require dosage adjustment.
lozenges, sublingual tablets/spray,
nasal spray (additional): Manage- INTERACTIONS
ment of acute or postoperative pain, pts DRUG: Strong CYP3A4 inhibitors (e.g.,
who are not opioid tolerant. GI obstruc- clarithromycin, ketoconazole, ritona-
tion, significant respiratory depression vir), cimetidine may increase concentra-
(Actiq, Fentora only), acute or severe tion/effect; risk for respiratory depression.
bronchial asthma. Cautions: Bradycardia; Strong CYP3A4 inducers (e.g., carBA-
renal, hepatic, respiratory disease; head Mazepine, phenytoin, rifAMPin) may
injuries; altered LOC; biliary tract disease; decrease concentration/effect. Alcohol,
acute pancreatitis; cor pulmonale; signifi- CNS depressants (e.g., LORazepam,
cant COPD; increased ICP; use of MAOIs haloperidol, zolpidem) may increase
within 14 days; elderly; morbid obesity. CNS depression. May increase serotonergic
effect of MAOIs (e.g., phenelzine, sele-
ACTION giline). HERBAL: Herbals with sedative
Binds to opioid receptors in CNS, reduc- properties (e.g., chamomile, kava kava,
ing stimuli from sensory nerve endings; valerian) may increase CNS depression.
inhibits ascending pain pathways. Ther- St. John’s wort may decrease concentra-
apeutic Effect: Alters pain reception, tion/effect. FOOD: None known. LAB VAL-
increases pain threshold. UES: May increase serum amylase, lipase.

PHARMACOKINETICS AVAILABILITY (Rx)


Route Onset Peak Duration Buccal Tablet: (Fentora):100 mcg, 200
IV 1–2 min 3–5 min 0.5–1 hr mcg, 400 mcg, 600 mcg, 800 mcg. Buc-
IM 7–15 min 20–30 min 1–2 hrs cal Soluble Film: (Onsolis): 200 mcg,
Transder­ 6–8 hrs 24 hrs 72 hrs 400 mcg, 600 mcg, 800 mcg, 1,200 mcg.
mal Injection Solution: 50 mcg/mL. Nasal
Transmu­ 5–15 min 20–30 min 1–2 hrs Spray: (Lazanda): 100 mcg/spray, 300
cosal mcg/spray, 400 mcg/spray. Sublingual
Well absorbed after IM or topical admin- Tablets: (Abstral): 100 mcg, 200 mcg,
istration. Transmucosal form absorbed 300 mcg, 400 mcg, 600 mcg, 800 mcg.
through buccal mucosa and GI tract. Pro- Sublingual Spray: (Subsys): 100 mcg,
tein binding: 80%–85%. Metabolized in 200 mcg, 400 mcg, 600 mcg, 800 mcg.

underlined – top prescribed drug


fentaNYL 483
Transdermal Patch: (Duragesic):12 mcg/ Sublingual Spray
hr, 25 mcg/hr, 50 mcg/hr, 75 mcg/hr, • Open blister pack with scissors im-
100 mcg/hr. Transmucosal Lozenges: mediately prior to use. • Spray con-
(Actiq): 200 mcg, 400 mcg, 600 mcg, 800 tents underneath tongue.
mcg, 1,200 mcg, 1,600 mcg.
Sublingual Tablets
ADMINISTRATION/HANDLING • Place under tongue. • Dissolves rap-
idly. • Do not suck, chew, or swallow
IV tablet.
Rate of administration • Give by slow F
Nasal
IV injection (over 1–2 min). • Too-rapid
injection increases risk of severe adverse • Prime device before use by spraying
reactions (skeletal/thoracic muscle rigidity into pouch. • Insert nozzle about 12
resulting in apnea, laryngospasm, broncho- inch into nose, pointing toward bridge of
spasm, peripheral circulatory collapse, nose, tilting bottle slightly. • Press
anaphylactoid effects, cardiac arrest). down firmly until hearing a “click” and
Storage • Store parenteral form at
number on counting window advances by
room temperature. • Opiate antagonist one. Do not blow nose for at least 30 min
(naloxone) should be readily available. following administration.
Transmucosal
Transdermal
• Apply to hairless area of intact skin of • Suck lozenge vigorously. • Allow to
upper torso. • Use flat, nonirritated dissolve over 15 min. • Do not chew.
site. • Firmly press evenly and hold for 30 IV INCOMPATIBILITIES
sec, ensuring that adhesion is in full contact
with skin and that edges are completely Azithromycin (Zithromax), pantoprazole
sealed. • Use only water to cleanse site (Protonix), phenytoin (Dilantin).
before application (soaps, oils may irritate IV COMPATIBILITIES
skin). • Rotate sites of applica-
tion. • Carefully fold used patches so that Atropine, bupivacaine (Marcaine, Sen-
system adheres to itself; discard in toi- sorcaine), cloNIDine (Duraclon), dex-
let. • If patch becomes loose, cover with a medetomidine (Precedex), dilTIAZem
transparent adhesive dressing; if patch (Cardizem), diphenhydrAMINE (Bena-
comes off, apply new patch, rotating sites dryl), DOBUTamine (Dobutrex), DOPa-
(this starts a new dosing interval). Normal mine (Intropin), droperidol (Inapsine),
exposure to water may loosen the adhesive. heparin, HYDROmorphone (Dilau-
did), ketorolac (Toradol), LORazepam
Buccal Film (Ativan), metoclopramide (Reglan),
• Wet inside of cheek. • Place film inside midazolam (Versed), milrinone (Pri-
mouth with pink side of unit against macor), morphine, nitroglycerin, nor-
cheek. • Press film against cheek and hold epinephrine (Levophed), ondansetron
for 5 sec. • Leave in place until dissolved (Zofran), potassium chloride, propofol
(15–30 min). • Do not chew, swallow, cut (Diprivan).
film. • Liquids may be given after 5 min of
application; food after film dissolves. INDICATIONS/ROUTES/DOSAGE
Note: Doses titrated to desired effect
Buccal Tablets dependent upon degree of analgesia, pt
• Place tablet above a rear molar be- status.
tween upper cheek and gum. • Dis-
solve over 30 min. • Swallow remain- Acute Pain Management (FentaNYL)
ing pieces with water. • Do not split IM/IV: ADULTS, ELDERLY: 0.35–0.5 mcg/
tablet. kg q30-60 min as needed.

Canadian trade name Non-Crushable Drug High Alert drug


484 fentaNYL
Continuous IV Infusion (FentaNYL) SIDE EFFECTS
ADULTS, ELDERLY: 0.7–10 mcg/kg/hr. Frequent: IV: Postop drowsiness, nau-
Usual Buccal Dose (Fentora) sea, vomiting. Transdermal (10%–
ADULTS, ELDERLY: Initially, 100 mcg. Titrate 3%): Headache, pruritus, nausea,
dose up to 800 mcg single dose, providing vomiting, diaphoresis, dyspnea, confu-
adequate analgesia with tolerable side effects. sion, dizziness, drowsiness, diarrhea,
constipation, decreased appetite. Occa-
Usual Buccal Soluble Film Dose (Onsolis) sional: IV: Postop confusion, blurred
Note: All pts must initiate with 200 mcg. vision, chills, orthostatic hypotension,
F constipation, difficulty urinating. Trans-
ADULTS, ELDERLY: Initially, 200 mcg up to
1,200 mcg. Maximum: No more than 4 dermal (3%–1%): Chest pain, arrhyth-
doses/day; separate by at least 2 hrs. mias, erythema, pruritus, syncope,
agitation, skin irritations.
Usual Nasal Dose (Lazanda)
Nasal: ADULTS, ELDERLY: Initially, 100 ADVERSE EFFECTS/TOXIC
mcg. Titrate from 100 mcg to 200 mcg to REACTIONS
300 mcg to 400 mcg to 600 mcg to 800 mcg Overdose or too-rapid IV administration
(maximum). Wait at least 2 hrs between may produce severe respiratory depres-
doses; no more than 4 doses in 24 hrs. sion, skeletal/thoracic muscle rigidity
(may lead to apnea, laryngospasm, bron-
Usual Sublingual Tablet Dose (Abstral) chospasm, cold/clammy skin, cyanosis,
ADULTS, ELDERLY: Initially, 100 mcg, then coma). Tolerance to analgesic effect
titrate to 400 mcg in 100 mcg increments, may occur with repeated use. Antidote:
then in 200 mcg increments to 600 mcg Naloxone (see Appendix J for dos-
up to 800 mcg. Wait at least 2 hrs between age). Abrupt stoppage of prolonged high-
doses; no more than 4 doses in 24 hrs. dose, continuous infusions may induce
opiate withdrawal.
Usual Sublingual Spray Dose (Subsys)
ADULTS, ELDERLY: Initially, 100 mcg. May NURSING CONSIDERATIONS
repeat with same dose in 30 min if pain
not relieved. Must wait at least 4 hours BASELINE ASSESSMENT
before treating another episode of pain. Resuscitative equipment, opiate an-
May titrate to 200 mcg to 400 mcg to 600 tagonist (naloxone 0.5 mcg/kg) should
mcg to 800 mcg to 1200 mcg to 1600 mcg. be available for initial use. Establish
baseline B/P, respirations. Assess type,
Usual Transdermal Dose (Duragesic) location, intensity, duration of pain. De-
ADULTS, ELDERLY, CHILDREN 12 YRS AND termine daily morphine equivalency in
OLDER: Initially, 12–25 mcg/hr. May cancer pts who are being transitioned to
increase after 3 days. chronic therapy.
Usual Transmucosal Dose (Actiq) INTERVENTION/EVALUATION
ADULTS, CHILDREN: 200–1200 mcg for Assist with ambulation. Encourage po-
breakthrough pain. Limit to 4 applica- stop pt to turn, cough, deep breathe
tions/day. Titrate to provide adequate anal- q2h. Monitor respiratory rate, B/P, heart
gesia while minimizing adverse effects. rate, oxygen saturation. Assess for relief
of pain. In pts with prolonged high-
Dosage in Renal/Hepatic Impairment
dose, continuous infusions (critical
Injection: No dose adjustment.
care, ventilated pts), consider weaning
Transdermal patch: Mild to moder-
drip gradually or transition to a fentanyl
ate impairment: Reduce dose by 50%.
patch to decrease symptoms of opiate
Severe impairment: Not recommended.
withdrawal.

underlined – top prescribed drug


ferric gluconate 485
PATIENT/FAMILY TEACHING PRECAUTIONS
• Avoid alcohol; do not take other med- Contraindications: Hypersensitivity to
ications without consulting physi- iron salts. Hemochromatosis, hemolytic
cian. • Avoid tasks that require alert- anemias. Cautions: Peptic ulcer, regional
ness, motor skills until response to drug enteritis, ulcerative colitis, pts receiving
is established. • Teach pt proper trans- frequent blood transfusions.
dermal, buccal, lozenge administra-
tion. • Transdermal: Avoid saunas ACTION
(increases drug release time). • Use as Essential component in formation of Hgb,
directed to avoid overdosage; potential myoglobin, enzymes. Promotes effective F
for physical dependence with prolonged erythropoiesis and transport, utilization
use. • Report constipation, absence of of oxygen. Therapeutic Effect: Pre-
pain relief. • Taper slowly after long- vents iron deficiency.
term use.
PHARMACOKINETICS
Absorbed in duodenum and upper jeju-
num. Ten percent absorbed in pts with nor-
ferric gluconate mal iron stores; increased to 20%–30% in
pts with inadequate iron stores. Primarily
fer-ick gloo-koe-nate bound to serum transferrin. Excreted
(Ferrlecit) in urine, sweat, sloughing of intestinal
mucosa, menses. Half-life: 6 hrs.
ferrous fumarate LIFESPAN CONSIDERATIONS
fer-us fue-ma-rate Pregnancy/Lactation: Crosses placenta;
(Ferrocite, Palafer ) distributed in breast milk. Children/
Elderly: No age-related precautions
noted.
ferrous gluconate
INTERACTIONS
fer-us gloo-koe-nate DRUG: Antacids may decrease absorp-
(Apo-Ferrous Gluconate , Ferate) tion of ferrous compounds. May decrease
absorption of bisphosphonates (e.g.,
ferrous sulfate risedronate), cefdinir, quinolones,
tetracyclines. HERBAL: None significant.
fer-us sul-fate FOOD: Cereal, coffee, dietary fiber,
(Fer-In-Sol, Fer-Iron, Slow-Fe) eggs, milk, tea decrease absorption. LAB
VALUES: May increase serum bilirubin,
uCLASSIFICATION iron. May decrease serum calcium.
PHARMACOTHERAPEUTIC: Enzymat-
ic mineral. CLINICAL: Iron prepara- AVAILABILITY (OTC)
tion. Ferric Gluconate
Injection, solution: 12.5 mg/mL.
Ferrous Fumarate
USES Tablets: 90 mg (29.5 mg elemental
Ferrous fumarate, gluconate, sulfate: iron), 324 mg (106 mg elemental iron).
Prevention, treatment of iron-deficiency
anemia. Ferric gluconate: Treatment Ferrous Gluconate
of iron-deficiency anemia in combination Tablets: 240 mg (27 mg elemental iron)
with erythropoietin in HD pts. (Fergon), 325 mg (36 mg elemental iron).

Canadian trade name Non-Crushable Drug High Alert drug


486 ferric gluconate
Ferrous Sulfate mL (50 mg elemental iron/mL) = 0.0442
Oral Solution: 75 mg/mL (15 mg/mL (desired Hgb less observed Hgb) × lean
elemental iron). Tablets: 325 mg (65 body weight (in kg) + (0.26 × lean body
mg elemental iron). Syrup: 300 mg/5 mL weight). Give 2 mL or less once daily until
(60 mg elemental iron per 5 mL). total dose reached. CHILDREN WEIGHING
Tablets (Timed-Release): 160 mg 5–15 KG: Dose in mL (50 mg elemental iron/
(50 mg elemental iron). mL) = 0.0442 (desired Hgb less observed
Hgb) × body weight (in kg) + (0.26 × body
ADMINISTRATION/HANDLING weight). Give 2 mL or less once daily until
F PO total dose reached.
• Store all forms (tablets, capsules, sus- IV: ADULTS, ELDERLY (HEMODIALYSIS-DEPEN-
pension, drops) at room tempera- DENT PTS): 5 mL iron sucrose (100 mg
ture. • Ideally, give between meals with elemental iron) delivered during dialysis;
water or juice but may give with meals if administer 1–3 times/wk to total dose of
GI discomfort occurs. • Transient 1,000 mg in 10 doses. Give no more than
staining of mucous membranes, teeth 3 times/wk. CHILDREN 2 YRS AND OLDER: 0.5
occurs with liquid iron preparation. To mg/kg/dose (maximum: 100 mg) q2wks
avoid staining, place liquid on back of for 6 doses. (PERITONEAL DIALYSIS–DEPEN-
tongue with dropper or straw. • Do not DENT PTS): Two infusions of 300 mg over 90
give with milk or milk products. • Do min 14 days apart, followed by a single 400-
not break, crush, dissolve, or divide mg dose over 2.5 hrs 14 days later. CHIL-
timed-release tablets. DREN 2 YRS AND OLDER: 0.5 mg/kg/dose
(maximum: 100 mg) q4wks for 3 doses.
INDICATIONS/ROUTES/DOSAGE (NON–DIALYSIS-DEPENDENT PTS): 200
Iron-Deficiency Anemia mg over 2–5 min on 5 different occa-
Dosage is expressed in terms of milli- sions within 14 days. CHILDREN 2 YRS AND
grams of elemental iron. Assess degree of OLDER: 0.5 mg/kg/dose (maximum: 100
anemia, pt weight, presence of any bleed- mg) q4wks for 3 doses.
ing. Expect to use periodic hematologic
Prevention of Iron Deficiency
determinations as guide to therapy.
PO: (Ferrous Fumarate): ADULTS,
IV: (Ferric Gluconate): ADULTS,
ELDERLY: 30–60 mg/day. CHILDREN:
ELDERLY: 125 mg/dose. Usual dose: 1,000
(5–12 yrs): 30–60 mg/day. (2–4 yrs): 30 mg/
mg given over 8 sessions.
PO: (Ferrous Fumarate): ADULTS,
day. (6 mos–1 yr): 10–12.5 mg/day. (Ferrous
Gluconate): ADULTS, ELDERLY: 30–60 mg/
ELDERLY: 65–200 mg/day in 2–3 divided
doses. CHILDREN: 3–6 mg/kg/day in 2–3 day. CHILDREN: (5–12 yrs): 30–60 mg/day.
(2–4 yrs): 30 mg/day. (6 mos–1 yr): 10–12.5
divided doses. (Ferrous Gluconate):
ADULTS, ELDERLY: 65–200 mg/day in 2–3
mg/day. (Ferrous Sulfate): ADULTS,
ELDERLY: 30–60 mg/day. CHILDREN: (5–12
divided doses. CHILDREN: 3–6 mg/kg/day
yrs): 30–60 mg/day. (2–4 yrs): 30 mg/day. (6
in 2–3 divided doses. (Ferrous Sulfate):
mos–1 yr): 10–12.5 mg/day.
ADULTS, ELDERLY: 65–200 mg/day in 2–3
divided doses. CHILDREN: 3–6 mg/kg/day SIDE EFFECTS
in 2–3 divided doses.
IV: (Iron Dextran): ADULTS, ELDERLY, CHIL- Occasional: Mild, transient nausea.
DREN WEIGHING MORE THAN 15 KG: Dose in Rare: Heartburn, anorexia, constipation,
mL (50 mg elemental iron/mL) = 0.0442 diarrhea.
(desired Hgb less observed Hgb) × lean
body weight (in kg) + (0.26 × lean body ADVERSE EFFECTS/TOXIC
weight). Give 2 mL or less once daily until REACTIONS
total dose reached. IV: ADULTS, ELDERLY, CHIL- Large doses may aggravate existing GI tract
DREN WEIGHING MORE THAN 15 KG: Dose in disease (peptic ulcer, regional enteritis,
underlined – top prescribed drug
fesoterodine 487
ulcerative colitis). Severe iron poisoning USES
occurs most often in children, manifested as Treatment of overactive bladder with
vomiting, severe abdominal pain, diarrhea, symptoms including urinary inconti-
dehydration, followed by hyperventilation, nence, urgency, frequency.
pallor, cyanosis, cardiovascular collapse.
PRECAUTIONS
NURSING CONSIDERATIONS Contraindications: Hypersensitivity to fes-
BASELINE ASSESSMENT oterodine. Gastric retention, uncontrolled
Assess nutritional status, dietary history. narrow-angle glaucoma, urinary retention.
Cautions: Severe renal impairment, severe F
Question history of hemochromatosis,
hemolytic anemia, ulcerative colitis. hepatic impairment, clinically significant
Question use of antacids, calcium supple- bladder outflow obstruction (risk of uri-
ments. nary retention), GI obstructive disorders
(e.g., pyloric stenosis [risk of gastric reten-
INTERVENTION/EVALUATION tion], treated narrow-angle glaucoma,
Monitor serum iron, total iron-binding myasthenia gravis, concurrent therapy with
capacity, reticulocyte count, Hgb, fer- strong CYP3A4 inhibitors, elderly, use in hot
ritin. Monitor daily pattern of bowel weather.
activity, stool consistency. Assess for
clinical improvement, record relief of ACTION
iron-deficiency symptoms (fatigue, irri- Exhibits antimuscarinic activity by interced-
tability, pallor, paresthesia of extremities, ing via cholinergic muscarinic receptors,
headache). thereby mediating urinary bladder contrac-
tion. Therapeutic Effect: Decreases uri-
PATIENT/FAMILY TEACHING nary frequency, urgency.
• Expect stool color to darken. • Oral
liquid may stain teeth. • To prevent mu- PHARMACOKINETICS
cous membrane and teeth staining with Well absorbed following PO adminis-
liquid preparation, use dropper or straw tration. Protein binding: 50%. Rapidly
and allow solution to drop on back of and extensively hydrolyzed to its active
tongue. • If GI discomfort occurs, take metabolite. Primarily excreted in urine.
after meals or with food. • Do not take Half-life: 7 hours.
within 2 hrs of other medication or eggs,
milk, tea, coffee, cereal. • Do not take LIFESPAN CONSIDERATIONS
antacids or OTC calcium supplements. Pregnancy/Lactation: Unknown if dis-
tributed in breast milk. Children: Safety and
efficacy not established. Elderly: Increased
incidence of antimuscarinic adverse events,
fesoterodine including dry mouth, constipation, dyspep-
sia; increase in residual urine, dizziness,
fes-oh-ter-oh-deen urinary tract infections higher in pts 75 yrs
(Toviaz) of age and older.
Do not confuse fesoterodine
with fexofenadine or toltero- INTERACTIONS
dine. DRUG: CYP3A4 inhibitors (e.g., clar-
ithromycin, ketoconazole, ritonavir)
uCLASSIFICATION may increase concentration/effect. Aclidin-
PHARMACOTHERAPEUTIC: Mus- ium, ipratropium, tiotropium, umecli-
carinic receptor antagonist. CLINI- dinium may increase anticholinergic effect.
CAL: Antispasmodic. Strong CYP3A4 inducers (e.g., carBA-
Mazepine, phenytoin, rifAMPin) may
Canadian trade name Non-Crushable Drug High Alert drug
488 fexofenadine
decrease concentration/effect. HERBAL: St. INTERVENTION/EVALUATION
John’s wort may decrease concentra- Assist with ambulation if dizziness oc-
tion/effect. FOOD: None known. LAB VAL- curs. Question for visual changes. Moni-
UES: May increase serum ALT, GGT. tor incontinence, postvoid residuals.
Monitor daily pattern of bowel activity,
AVAILABILITY (Rx) stool consistency.
Tablets, Extended-Release: 4 mg, 8 mg. PATIENT/FAMILY TEACHING
ADMINISTRATION/HANDLING • May produce constipation and urinary
F PO retention. • Blurred vision may occur;
• May be administered with or without use caution until drug effects have been
food. • Swallow whole; do not break, determined. • Heat prostration (due to
crush, dissolve, or divide tablet. decreased sweating) can occur if used in
a hot environment. • Do not ingest
INDICATIONS/ROUTES/DOSAGE grapefruit products.
Overactive Bladder
PO: ADULTS, ELDERLY: Initially, 4 mg once
daily. May increase to 8 mg once daily.
Maximum dose for pts with concurrent fexofenadine
use of strong CYP3A4 inhibitors (e.g., eryth-
romycin, ketoconazole) is 4 mg once daily. fex-oh-fen-a-deen
(Allegra Allergy, Allegra Allergy
Dosage in Renal Impairment Children’s)
PO: ADULTS, ELDERLY: Maximum: 4 mg Do not confuse Allegra with
with CrCl less than 30 mL/min. Viagra, or fexofenadine with
fesoterodine.
Dosage in Hepatic Impairment
Mild to moderate impairment: No FIXED-COMBINATION(S)
dose adjustment. Severe impairment: Allegra-D 12 Hour: fexofenadine/
Not recommended. pseudoephedrine (sympathomimetic):
SIDE EFFECTS 60 mg/120 mg. Allegra-D 24 Hour:
fexofenadine/pseudoephedrine (sym-
Frequent (34%–18%): Dry mouth. Occa- pathomimetic): 180 mg/240 mg.
sional (6%–3%): Constipation, urinary
tract infection, dry eyes. Rare (2% or uCLASSIFICATION
less): Nausea, dysuria, back pain, rash, PHARMACOTHERAPEUTIC: Hista-
insomnia, peripheral edema. mine H1 antagonist. CLINICAL: CLIN-
ADVERSE EFFECTS/TOXIC ICAL: Antihistamine.
REACTIONS
Severe anticholinergic effects including USES
abdominal cramps, facial warmth, exces-
sive salivation/lacrimation, diaphoresis, Relief of symptoms associated with hay-
pallor, urinary urgency, blurred vision. fever or other upper respiratory allergies
(e.g., runny nose, sneezing, itching of
NURSING CONSIDERATIONS nose/throat).
BASELINE ASSESSMENT PRECAUTIONS
Assess urinary pattern (e.g., urinary fre- Contraindications: Hypersensitivity to
quency, urgency). Obtain baseline chem- fexofenadine. Cautions: Renal impair-
istries. Question history as listed in Pre- ment, hypertension (if drug com-
cautions. Receive full medication history. bined with pseudoephedrine). Orally
underlined – top prescribed drug
fexofenadine 489
disintegrating tablet not recommended in ADMINISTRATION/HANDLING
children younger than 6 yrs. PO
• Give without regard to food. • Avoid
ACTION
giving with fruit juices (apple, grapefruit,
Competes with histamine-1 receptor site orange). Administer with water
on effector cells in GI tract, blood ves- only. • Shake suspension well before use.
sels, and respiratory tract. Therapeutic
Effect: Relieves hayfever/upper respira- PO (Orally Disintegrating Tablet)
tory symptoms. • Take on empty stomach. • Remove
from blister pack; immediately place on F
PHARMACOKINETICS tongue. • May take with or without liq-
Onset Peak Duration uid. • Do not split or cut.
PO 60 min — 12 hrs or greater INDICATIONS/ROUTES/DOSAGE
Rapidly absorbed after PO administration. Hayfever, Upper Respiratory Symptoms
Protein binding: 60%–70%. Does not cross PO: ADULTS, ELDERLY, CHILDREN 12 YRS
blood-brain barrier. Minimally metabolized. AND OLDER: 60 mg twice daily or 180
Excreted in feces (80%), urine (11%). Not mg once daily. CHILDREN 2–11 YRS: 30 mg
removed by hemodialysis. Half-life: 14.4 twice daily. (Suspension for ages 2–11
hrs (increased in renal impairment). yrs; ODT for ages 6–11 yrs).

LIFESPAN CONSIDERATIONS Dosage in Renal Impairment


PO: ADULTS, ELDERLY, CHILDREN 12 YRS
Pregnancy/Lactation: Unknown if drug AND OLDER: 60 mg once daily. CHILDREN
crosses placenta or is distributed in breast 2–11 YRS: 30 mg once daily. CHILDREN 6
milk. Children: Safety and efficacy not MOS–LESS THAN 2 YRS: 15 mg once daily.
established in pts younger than 12 yrs.
CrCl Adults Children
Elderly: No age-related precautions noted.
>50 mL/min No adjust­ No adjust­
INTERACTIONS ment ment
10–50 mL/min 60 mg q12-24h 60 mg q24h
DRUG: Aluminum- and magnesium- <10 mL/min 30 mg q24h 30 mg q24h
containing antacids may decrease
absorption. Aclidinium, ipratro- Dosage in Hepatic Impairment
pium, tiotropium, umeclidinium No dose adjustment.
may increase anticholinergic effect. CNS
depressants (e.g., alcohol, mor- SIDE EFFECTS
phine, oxyCODONE, zolpidem) may Rare (less than 2%): Drowsiness, head-
increase CNS depression. May increase ache, fatigue, nausea, vomiting, abdomi-
concentrations of erythromycin, keto- nal distress, dysmenorrhea.
conazole. HERBAL: Herbals with seda-
tive properties (e.g., chamomile, ADVERSE EFFECTS/TOXIC
kava kava, valerian) may increase CNS REACTIONS
depression. FOOD: Grapefruit products Hypersensitivity reaction occurs rarely.
may decrease concentration/effect. LAB
VALUES: May suppress wheal, flare reac-
NURSING CONSIDERATIONS
tions to antigen skin testing unless drug is BASELINE ASSESSMENT
discontinued at least 4 days before testing. Assess severity of congestion, rhinitis, ur-
AVAILABILITY (Rx) ticaria, watery eyes. If pt is having an al-
lergic reaction, obtain history of recently
Oral Suspension: 30 mg/5 mL. Tab- ingested foods, drugs, environmental
lets: 60 mg, 180 mg. Tablets (Orally Disin- exposure, emotional stress. Monitor rate,
tegrating): 30 mg. depth, rhythm, type of respiration; quality,
Canadian trade name Non-Crushable Drug High Alert drug
490 fidaxomicin

rate of pulse. Assess lung sounds for rhon- and efficacy not established. Elderly: No
chi, wheezing, rales. age-related precautions noted.

INTERVENTION/EVALUATION INTERACTIONS
Assess for therapeutic response; relief DRUG: None significant. HERBAL: None
from allergy: itching, red, watery eyes, known. FOOD: None significant. LAB
rhinorrhea, sneezing. VALUES: May increase serum ALT, AST,
bilirubin, alkaline phosphatase.
PATIENT/FAMILY TEACHING
F • Avoid tasks that require alertness, AVAILABILITY (Rx)
motor skills until response to drug is Tablets: 200 mg.
established. • Avoid alcohol during an-
tihistamine therapy. • Coffee, tea may ADMINISTRATION/HANDLING
help reduce drowsiness. • Do not take • Give without regard to food.
with any fruit juices.
INDICATIONS/ROUTES/DOSAGE
Clostridium Difficile–Associated Diarrhea
fidaxomicin PO: ADULTS: 200 mg twice daily for 10
days.
fye-dax-oh-mye-sin
Dosage in Renal/Hepatic Impairment
(Dificid)
No dose adjustment.
uCLASSIFICATION
SIDE EFFECTS
PHARMACOTHERAPEUTIC: Mac-
Frequent (62%–33%): Nausea, vomiting,
rolide. CLINICAL: Antibiotic.
abdominal pain. Rare (less than 2%): Pru-
ritus, rash.
USES
Treatment of C. difficile–associated diar­ ADVERSE EFFECTS/TOXIC
r­hea. REACTIONS
Less than 2% reported events most likely
PRECAUTIONS related to diarrhea-associated illness
Contraindications: Hypersensitivity to including volume loss, dehydration, GI
fidaxomicin. Cautions: History of ane- bleeding, bloating, megacolon, abdominal
mia, neutropenia, macrolide allergy. distention/tenderness, flatulence, dys-
pepsia, dysphagia, intestinal obstruction,
ACTION bicarbonate loss, hyperglycemia, metabolic
Binds to ribosomal sites of susceptible organ- acidosis, and increased hepatic function
isms, inhibiting RNA-dependent p­ rotein syn- tests. GI tract infection may cause bleeding,
thesis by RNA polymerase. Therapeutic decreased platelets, decreased RBC count.
Effect: Bactericidal against C. difficile.
NURSING CONSIDERATIONS
PHARMACOKINETICS BASELINE ASSESSMENT
Minimal systemic absorption following Verify positive C. difficile toxin test before
PO administration. Mainly confined to GI initiating treatment. Implement infection
tract. Excreted primarily in feces (92%). control measures. Obtain baseline CBC,
Half-life: 9 hrs. electrolytes, renal function, fecal occult
blood test. Assess abdominal pain, bowel
LIFESPAN CONSIDERATIONS sounds, and stool characteristics (color,
Pregnancy/Lactation: Unknown if dis- frequency, consistency). Assess hydration
tributed in breast milk. Children: Safety status.
underlined – top prescribed drug
filgrastim 491

INTERVENTION/EVALUATION severe neutropenia, fever. Neupogen,


Zarxio: Reduces neutropenia duration,
Monitor for volume loss, dehydration, sequelae in pts with nonmyeloid malig-
hypotension, abdominal pain, pyrexia. nancies having myeloablative therapy
Encourage nutrition/fluid intake. Moni- followed by bone marrow transplant
tor daily pattern of bowel activity, stool (BMT). Mobilization of hematopoietic
consistency. Routinely assess bowel progenitor cells into peripheral blood
sounds. Screen for intestinal obstruc- for collection by apheresis. Treatment of
tion (increased nausea, abdominal pain, chronic, severe neutropenia. Decreases
hyperactive bowel sounds) and consider incidence of infection in pts with malig- F
abdominal X-ray if suspected. nancies receiving chemotherapy asso-
PATIENT/FAMILY TEACHING ciated with increased incidence of
• Complete drug therapy, despite symp- severe neutropenia with fever. Reduces
tom improvement. Early discontinuation time to neutrophil recovery/duration
may result in antibacterial resistance and of fever after induction/consolidation
increased risk of recurrent infec- chemotherapy in AML pts. Neupogen:
tion. • Report weakness, fatigue, pale Increases survival in pts acutely exposed
skin, dizziness, or red/dark, tarry stools to myelosuppressive doses of radiation.
relating to GI bleeding. • C. difficile OFF-LABEL: Treatment of AIDS-related
infection is extremely contagious to oth- neutropenia in pts receiving zidovudine;
ers. Wash hands frequently with soap and drug-induced neutropenia; anemia in
water, esp. after bowel movements. C. myelodysplastic syndrome; hepatitis
difficile spores can live on objects for C virus infection treatment-associated
months. Use bleach products to cleanse neutropenia.
bathroom, doorknobs, other high-touch PRECAUTIONS
surfaces. If possible, use a separate bath-
room away from others. • Drink plenty Contraindications: Hypersensitivity to
of fluids. filgrastim. Neupogen, Zarxio (addi-
tional): History of serious allergic
reaction to human granulocyte colony-
stimulating factors. Cautions: Malig-
filgrastim nancy with myeloid characteristics (due
to G-CSF’s potential to act as growth fac-
fil-gras-tim tor), gout, psoriasis, neutrophil count
(Granix, Neupogen, Zarxio) greater than 50,000 cells/mm3, sickle
Do not confuse Neupogen with cell disease, concomitant use of other
Epogen, Neulasta, Neumega, or drugs that may result in thrombocyto-
Nutramigen. penia. Do not use 24 hrs before or after
cytotoxic chemotherapy.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Hemat-
ACTION
opoietic agent. CLINICAL: Granu- Stimulates production, maturation,
locyte colony-stimulating factor (G- activation of neutrophils. Therapeutic
CSF). Effect: Increases migration and cytotox-
icity of neutrophils.

USES PHARMACOKINETICS
Granix: Decreases duration of severe Readily absorbed. Onset of action: 24
neutropenia in adults and children 1 mo hrs (plateaus in 3–5 days). WBC return
and older with nonmyeloid malignancies to normal in 4–7 days. Not removed by
receiving chemotherapy associated with hemodialysis. Half-life: 3.5 hrs.
Canadian trade name Non-Crushable Drug High Alert drug
492 filgrastim

LIFESPAN CONSIDERATIONS SQ
• Aspirate syringe before injection
Pregnancy/Lactation: Unknown if
(avoid intra-arterial administration).
drug crosses placenta or is distributed in
Storage • Store in refrigerator, but
breast milk. Children/Elderly: No age-
remove before use and allow to warm to
related precautions noted.
room temperature.
INTERACTIONS IV INCOMPATIBILITIES
DRUG: May increase concentration/effects Amphotericin (Fungizone), cefepime (Maxi-
F of bleomycin, cyclophosphamide, pime), cefotaxime (Claforan), cefOXitin
topotecan. HERBAL: None significant. (Mefoxin), ceftizoxime (Cefizox), cefTRIAX-
FOOD: None known. LAB VALUES: May one (Rocephin), clindamycin (Cleocin),
increase LDH, leukocyte alkaline phos- DACTINomycin (Cosmegen), etoposide (Ve-
phatase (LAP) scores, serum alkaline Pesid), fluorouracil, furosemide (Lasix),
phosphatase, uric acid. heparin, mannitol, methylPREDNISolone
(Solu-Medrol), mitoMYcin (Mutamycin),
AVAILABILITY (Rx) prochlorperazine (Compazine).
Injection Solution: (Neupogen): 300 mcg/
mL, 480 mcg/1.6 mL Injection, Prefilled IV COMPATIBILITIES
Syringe: (Granix, Neupogen, Zarxio): 300 Bumetanide (Bumex), calcium gluco-
mcg/0.5 mL, 480 mcg/0.8 mL. nate, HYDROmorphone (Dilaudid),
LORazepam (Ativan), morphine, potas-
ADMINISTRATION/HANDLING sium chloride.
b ALERT c May be given by SQ injec- INDICATIONS/ROUTES/DOSAGE
tion, short IV infusion (15–30 min), or
b ALERT c Begin therapy at least 24 hrs
continuous IV infusion. Do not dilute
after last dose of chemotherapy and at
with normal saline.
least 24 hrs after bone marrow infusion.
IV Dosing based on actual body weight.
Reconstitution • Allow vial to warm Chemotherapy-Induced Neutropenia
to room temperature (approx. 30 Neupogen, Zarxio
mins). • Visually inspect for particulate IV or SQ infusion, SQ injection:
matter or discoloration. • Dilute in ADULTS, ELDERLY, CHILDREN: Initially, 5 mcg/
D5W from concentration of 300 mcg/mL kg/day. May increase by 5 mcg/kg for each
to 5 mcg/mL (do not dilute to a final chemotherapy cycle based on duration/
concentration less than 5 mcg/mL). Di- severity of neutropenia; continue for up to
luted solutions of 5–15 mcg/mL should 14 days or until absolute neutrophil count
have addition of albumin to a final con- (ANC) reaches 10,000 cells/mm3.
centration of 2 mg/mL. • Do not dilute Granix
with saline. SQ: ADULTS, ELDERLY: 5 mcg/kg/day.
Rate of administration • For inter- Continue until nadir has passed and neu-
mittent infusion (piggyback), infuse over trophil count recovered to normal range.
15–30 min. • For continuous infusion,
give single dose over 4–24 hrs. • In all Bone Marrow Transplant
situations, flush IV line with D5W before IV or SQ infusion: (Neupogen,
and after administration. Zarxio): ADULTS, ELDERLY, CHILDREN: 10
Storage • Refrigerate vials and sy- mcg/kg/day. Administer >24 hrs after
ringes. • Stable for up to 24 hrs at chemotherapy or bone marrow transfu-
room temperature (provided vial con- sion. Adjust dosage daily during period of
tents are clear and contain no particulate neutrophil recovery based on neutrophil
matter). response.
underlined – top prescribed drug
finasteride 493
Mobilization of Progenitor Cells leukocytosis, MI, thrombocytopenia,
IV or SQ infusion: (Neupogen, sickle cell crisis, splenic rupture may
Zarxio): ADULTS: 10 mcg/kg/day in occur.
donors beginning at least 4 days before
first leukapheresis and continuing until NURSING CONSIDERATIONS
last leukapheresis (usually for 6–7 BASELINE ASSESSMENT
days). Discontinue for WBC greater than
100,000 cells/mm3. CBC, platelet count should be obtained
before therapy initiation and twice wkly
Chronic Neutropenia, thereafter. F
Congenital Neutropenia
INTERVENTION/EVALUATION
SQ: (Neupogen, Zarxio): ADULTS,
CHILDREN: Initially, 6 mcg/kg/dose twice In septic pts, be alert for adult respiratory
daily. Adjust dose based on ANC/clinical distress syndrome. Closely monitor those
response. with preexisting cardiac conditions.
Monitor B/P (transient decrease in B/P
Idiopathic or Cyclic Chronic Neutropenia may occur), temperature, CBC with dif-
SQ: (Neupogen, Zarxio): ADULTS, ferential, platelet count, serum uric acid,
CHILDREN: Initially, 5 mcg/kg/dose once hepatic function tests.
daily. Adjust dose based on ANC/clinical PATIENT/FAMILY TEACHING
response.
• Report fever, chills, severe bone pain,
Radiation Injury Syndrome chest pain, palpitations, difficulty breath-
SQ: ADULTS, ELDERLY: 10 mcg/kg once ing; left upper abdominal pain/tightness;
daily. Continue until ANC remains greater flank pain.
than 1,000 cells/mm3 for 3 consecutive
CBCs or ANC exceeds 10,000 cells/mm3
after radiation-induced nadir.
finasteride
Dosage in Renal/Hepatic Impairment
No dose adjustment. fin-as-ter-ide
(Propecia, Proscar)
SIDE EFFECTS Do not confuse finasteride with
Frequent (57%–11%): Nausea/vomiting, furosemide, or Proscar with
mild to severe bone pain (more fre- ProSom, Provera, or PROzac.
quent with high-dose IV form, less fre-
quent with low-dose SQ form), alopecia, uCLASSIFICATION
diarrhea, fever, fatigue. Occasional PHARMACOTHERAPEUTIC: 5-alpha-
(9%–5%): Anorexia, dyspnea, headache, reductase inhibitor. CLINICAL: Be-
cough, rash. Rare (less than 5%): Psoria- nign prostatic hyperplasia agent.
sis, hematuria, proteinuria, osteoporosis.

ADVERSE EFFECTS/TOXIC USES


REACTIONS Proscar: Treatment (monotherapy) of
Long-term administration occasionally symptomatic benign prostatic hyper-
produces chronic neutropenia, sple- plasia (BPH) to improve symptoms,
nomegaly. Acute respiratory distress reduce risk of acute urinary retention,
syndrome, alveolar hemorrhage and or reduce the need for surgery, includ-
hemoptysis (pts undergoing peripheral ing transurethral resection of the pros-
blood progenitor cell collection mobi- tate (TURP) and prostatectomy. Used in
lization), capillary leak syndrome, cuta- combination with an alpha-blocker (e.g.,
neous vasculitis, glomerulonephritis, doxazosin) to reduce risk of symptomatic
Canadian trade name Non-Crushable Drug High Alert drug
494 finasteride
progression. Propecia: Treatment of follicle-stimulating hormone (FSH),
male pattern hair loss. OFF-LABEL: Treat- luteinizing hormone (LH), testosterone.
ment of female hirsutism.
AVAILABILITY (Rx)
PRECAUTIONS Tablets: 1 mg (Propecia), 5 mg
Contraindications: Hypersensitivity to fin- (Proscar).
asteride, pregnancy or women of child-
bearing potential. Cautions: Hepatic ADMINISTRATION/HANDLING
impairment, urinary outflow obstruc- PO
F tion, urinary retention. Women who • Do not break, crush, dissolve, or di-
are attempting to conceive should avoid vide film-coated tablets. • Give without
exposure to crushed or broken tablets. regard to food.
ACTION INDICATIONS/ROUTES/DOSAGE
Inhibits 5-alpha reductase, an intracellular Benign Prostatic Hyperplasia (BPH)
enzyme that converts testosterone into dihy- PO: ADULTS, ELDERLY: (Proscar): 5 mg
drotestosterone (DHT) in prostate gland, once daily. Use as single agent or in combi-
resulting in decreased serum DHT. Thera- nation with doxazosin (6–12 mos of treat-
peutic Effect: Reduces size of prostate ment usually needed to assess benefit).
gland.
Hair Loss
PHARMACOKINETICS PO: ADULTS: (Propecia): 1 mg/day
Route Onset Peak Duration (Continue for at least 12 mos to assess
PO (reduction 8 hrs — 24 hrs full benefit).
of DHT)
Dosage in Renal Impairment
Rapidly absorbed from GI tract. Protein No dose adjustment.
binding: 90%. Widely distributed. Metab-
olized in liver. Half-life: 6–8 hrs. Onset Dosage in Hepatic Impairment
of clinical effect: 3–6 mos of continued Use caution.
therapy.
SIDE EFFECTS
LIFESPAN CONSIDERATIONS Rare (4%–2%): Gynecomastia, sexual
Pregnancy/Lactation: Physical han- dysfunction (impotence, decreased
dling of tablet by those who are or may libido, decreased volume of ejaculate).
become pregnant may produce abnor-
malities of external genitalia of male fetus. ADVERSE EFFECTS/TOXIC
Children: Not indicated for use in chil-
REACTIONS
dren. Elderly: No age-related precautions Hypersensitivity reaction, circumoral
noted. swelling, testicular pain occur rarely.
NURSING CONSIDERATIONS
INTERACTIONS
DRUG: None significant. HERBAL: St. BASELINE ASSESSMENT
John’s wort may decrease concen- Digital rectal exam, serum prostate-specific
tration. Avoid concurrent use with antigen (PSA) determination should be per-
saw palmetto (not adequately stud- formed in pts with benign prostatic hyper-
ied). FOOD: None known. LAB VAL- plasia (BPH) before initiating therapy and
UES: Decreases serum prostate-specific periodically thereafter. Assess usual urinary
antigen (PSA) level, even in presence characteristics (frequency, ability to empty
of prostate cancer. Decreases dihy- bladder, urinary flow). Assess degree of uri-
drotestosterone (DHT). Increases nary retention with baseline bladder scan.
underlined – top prescribed drug
fingolimod 495
INTERVENTION/EVALUATION unstable angina, stroke, TIA, decompen-
Diligently monitor I&O, esp. in pts with sated requiring hospitalization or NYHA
large residual urinary volume, severely class III/IV HF. Cautions: Concomitant
diminished urinary flow, or obstructive use of antiarrhythmics, beta blockers,
uropathy. Obtain periodic bladder scan calcium channel blockers, immunosup-
to assess treatment effectiveness (or to pressants, immune modulators, anti-
assess for acute urinary retention). neoplastics, QT interval–prolonging
medications (e.g., amiodarone, cipro-
PATIENT/FAMILY TEACHING floxacin); bradycardia, severe hepatic
• Treatment may cause impotence, de- impairment, ischemic heart disease, dia- F
creased volume of ejaculate. • May not betes, hypokalemia, hypomagnesemia;
notice improved urinary flow even if history of syncope, uveitis; pts at risk for
prostate gland shrinks. • Must take developing bradycardia or heart block.
medication longer than 6 mos, and it is
unknown if medication decreases need ACTION
for surgery. • Because of potential risk Blocks capacity of lymphocytes to move
to male fetus, women who are or may out from lymph nodes, reducing num-
become pregnant should not handle tab- ber of lymphocytes available to the
lets or be exposed to pt’s semen. • Im- CNS. Therapeutic Effect: May involve
mediately report inability to urinate or reduction of lymphocyte migration into
severe bladder pain. central nervous system, which reduces
central inflammation.
PHARMACOKINETICS
fingolimod Metabolized by the enzyme sphingo-
sine kinase to active metabolite. Highly
fin-goe-li-mod distributed in red blood cells (85%).
(Gilenya) Minimally metabolized in liver. Protein
binding: 99.7%. Primarily excreted in
uCLASSIFICATION
urine. Half-life: 6–9 days.
PHARMACOTHERAPEUTIC: Sphin-
gosine 1-phosphate (S1P) receptor LIFESPAN CONSIDERATIONS
modulator. CLINICAL: Multiple scle- Pregnancy/Lactation: May cause fetal
rosis agent. harm. Unknown if distributed in breast
milk. Children: Safety and efficacy not
established in pts younger than 18 yrs.
USES Elderly: Age-related severe hepatic
Treatment of pts 10 yrs and older with impairment may increase risk of adverse
relapsing forms of multiple sclerosis reactions.
(MS) to reduce frequency of clinical
exacerbations, delay accumulation of INTERACTIONS
physical disability. DRUG: Beta blockers (e.g., carvedilol,
metoprolol), calcium channel block-
PRECAUTIONS ers (e.g., dilTIAZem, verapamil),
Contraindications: Hypersensitivity to ceritinib, esmolol may increase risk
fingo­limod. Sick sinus syndrome, sec- of bradycardia. May increase effects of
ond-degree or higher conduction block QT interval–prolonging medications
(unless pt has functioning pacemaker). (e.g., amiodarone, azithromycin,
Baseline QT interval 500 msec or greater. ciprofloxacin, haloperidol). May
Concurrent use of class Ia or III antiar- increase toxic effects of leflunomide,
rhythmic. Recent (within 6 mos) MI, natalizumab. May decrease effect of
Canadian trade name Non-Crushable Drug High Alert drug
496 fingolimod
nivolumab, sipuleucel-T. May increase of skin cancer, lymphoma, basal cell
immunosuppressive effect of tofaci- carcinoma have been reported. Progres-
tinib, other immunosuppressants. sive multifocal leukoencephalopathy
May decrease therapeutic effect of vac- (PML) (weakness, paralysis, vision loss,
cines, increase toxic effects of live vac- aphasia, cognition impairment) may
cines. HERBAL: Echinacea may decrease occur. Neurotoxicity, posterior reversible
therapeutic effect. FOOD: None known. encephalopathy may evolve into cerebral
LAB VALUES: Expect decrease in neutro- hemorrhage, CVA. May increase risk of
phil count. May increase serum alkaline hypertension.
F phosphatase, ALT, AST, bilirubin, triglycer-
ides. May reduce diagnostic effect of Coc- NURSING CONSIDERATIONS
cidioides immitis skin test. BASELINE ASSESSMENT

AVAILABILITY (Rx) Obtain baseline CBC, serum chemistries


prior to initial treatment. At initial treat-
Capsules: 0.25 mg, 0.5 mg. ment (within first 4–6 hrs after dose),
medication reduces heart rate, AV con-
ADMINISTRATION/HANDLING duction, followed by progressive in-
PO crease after first day of treatment. Obtain
• May give without regard to food. baseline vitals, with particular attention
to pulse rate. Perform ophthalmologic
INDICATIONS/ROUTES/DOSAGE evaluation prior to treatment and 3–4
Multiple Sclerosis mos after initiation of treatment. Ques-
PO: ADULTS 18 YRS AND OLDER, tion medical history as listed in Precau-
ELDERLY: 0.5 mg once daily. CHILDREN tions. Obtain full medication history and
10 YRS AND OLDER, ADOLESCENTS WEIGH- screen for interactions.
ING MORE THAN 40 KG: 0.5 mg once daily.
WEIGHING 40 KG OR LESS: 0.25 mg once INTERVENTION/EVALUATION
daily. Monitor for bradycardia for 6 hrs after
first dose, then as appropriate. Periodi-
Dosage in Renal/Hepatic Impairment cally monitor CBC, serum chemistries,
Mild to moderate impairment: No particularly lymphocyte count (expected
dose adjustment. Severe impairment: to decrease approximately 80% from
Use caution. baseline with continued treatment).
Monitor for signs of systemic or lo-
SIDE EFFECTS cal infection. Diligently monitor for
Frequent (25%–10%): Headache, diar- hypersensitivity reaction, neurological
rhea, back pain, cough. Occasional changes, symptoms of posterior revers-
(8%–5%): Dyspnea, clinical depression, ible encephalopathy (altered mental
dizziness, hypertension, migraine, par- status, seizures, visual disturbances),
esthesia, decreased weight. Rare (4%– PML, QT interval prolongation. Assess for
2%): Blurred vision, alopecia, eye pain, new skin lesions, malignancies. Conduct
asthenia, eczema, pruritus. ophthalmologic exams q3–4 mos after
initiation, during treatment, and with any
ADVERSE EFFECTS/TOXIC changes in vision.
REACTIONS
May increase risk of infections (influ- PATIENT/FAMILY TEACHING
enza, herpes viral infection, bronchitis, • Obtain regular eye examinations during
sinusitis, gastroenteritis, ear infection) and for 2 mos following treatment. • Use
in 13%–4% of pts. Pts with diabetes or effective methods of contraception during
history of uveitis are at increased risk and for 3 mos following treatment. • Im-
for developing macular edema. Cases mediately report neurological changes
underlined – top prescribed drug
fluconazole 497
such as confusion, severe headache, sei- to other triazoles (e.g., itraconazole, ter-
zure activity, vision changes, trouble conazole), imidazoles (e.g., butoconazole,
speaking, one-sided weakness, paraly- ketoconazole). Medications or conditions
sis. • Treatment may increase risk of known to cause arrhythmias.
certain cancers; report new skin lesions,
fever, chills, night sweats, generalized ACTION
weakness, weight loss, or pain or swelling Interferes with fungal cytochrome
of the lymph nodes. • Report allergic P-450 activity, an enzyme necessary for
reactions such as itching, rash, swelling of ergosterol formation (principal sterol
the face or tongue. • Report symptoms in fungal cell membrane). Thera- F
of infection, visual changes, yellowing peutic Effect: Directly damages fun-
of skin, eyes, dark urine. • Due to high gal membrane, altering its function.
risk for drug interactions, do not take Fungistatic.
newly prescribed medication unless ap-
proved by prescriber who originally PHARMACOKINETICS
started treatment. Well absorbed from GI tract. Widely dis-
tributed, including to CSF. Protein bind-
ing: 11%. Partially metabolized in liver.
Excreted unchanged primarily in urine.
fluconazole Partially removed by hemodialysis. Half-
life: 20–30 hrs (increased in renal
flu-kon-a-zole impairment).
(Diflucan)
Do not confuse Diflucan LIFESPAN CONSIDERATIONS
with diclofenac, Diprivan, or Pregnancy/Lactation: Secreted in
disulfiram, or fluconazole with hum­an breast milk. Use caution in
itraconazole, ketoconazole, breastfeeding females. Children: No
omeprazole, or pantoprazole. age-related pre­cautions noted. Elder-
ly: Age-related renal impairment may
uCLASSIFICATION require dosage adjust­ment.
PHARMACOTHERAPEUTIC: Synthetic
azole. CLINICAL: Antifungal agent. INTERACTIONS
DRUG: May increase concentration/
effect of budesonide, calcium chan-
USES nel blockers (e.g., amlodipine, nife-
Antifungal prophylaxis in pts undergo- dipine, verapamil), cyclosporine,
ing bone marrow transplant; candidia- ivabradine, methadone, rifabutin,
sis (esophageal, oropharyngeal, urinary sirolimus, tacrolimus, tofacitinib.
tract, vaginal); systemic Candida infec- May decrease effect of Saccharomyces
tions (e.g., candidemia); treatment of boulardii. May increase concentration/
cryptococcal meningitis. OFF-LABEL: effect, risk of myopathy of HMG-CoA
Cryptococcal pneumonia, candidal reductase inhibitors (e.g., atorv-
intertrigo. astatin, simvastatin). HERBAL: None
significant. FOOD: None known. LAB
PRECAUTIONS VALUES: May increase serum alkaline
Contraindications:Hypersensitivity to flu- phosphatase, bilirubin, ALT, AST.
conazole. Concomitant administration of
QT-prolonging medications (e.g., erythro- AVAILABILITY (Rx)
mycin, pimozide). Cautions: Hepatic/renal 200 mg
Injection, Solution, Pre-Mix:
impairment, hypokalemia, hypersensitivity (100 mL), 400 mg (200 mL). Powder

Canadian trade name Non-Crushable Drug High Alert drug


498 fluconazole
for Oral Suspension: 10 mg/mL, 40 mg/ Usual Dosage
mL. Tablets: 50 mg, 100 mg, 150 mg, Note: Duration and dose dependent on
200 mg. location/severity of infection.
PO/IV: ADULTS, ELDERLY: 150 mg once
ADMINISTRATION/HANDLING or loading dose: 200–800 mg. Main-
IV
tenance dose: 200–800 mg once
daily. CHILDREN AND NEONATES: Load-
Rate of administration • Do not ex- ing dose: 6–12 mg/kg. Maintenance
ceed maximum flow rate of 200 mg/hr. dose: 3–12 mg/kg once daily. Maxi-
F Storage • Store at room tempera- mum: 600 mg/day.
ture. • Do not remove from outer wrap
until ready to use. • Squeeze inner bag Dosage in Renal Impairment
to check for leaks. • Do not use paren- After a loading dose of 400 mg,
teral form if solution is cloudy, precipi- daily dosage is based on creatinine
tate forms, seal is not intact, or it is dis- clearance.
colored. • Do not add supplementary
medication. Creatinine
Clearance Dosage
PO Greater than 50 100%
• Give without regard to food. mL/min
50 mL/min or less 50%
IV INCOMPATIBILITIES Dialysis 50%
Amphotericin B (Fungizone), ampho- CCRT 400–800 mg as
tericin B complex (Abelcet, AmBisome, loading dose
Amphotec), ampicillin (Polycillin), cal- CVVH then 200–800 mg/day
CVVHDF 400–800 mg as
cium gluconate, cefotaxime (Claforan), loading dose, then
cefTRIAXone (Rocephin), cefuroxime 400–800 mg/day
(Zinacef), chloramphenicol (Chlo-
romycetin), clindamycin (Cleocin), Dosage in Hepatic Impairment
co-trimoxazole (Bactrim), diazePAM Use caution.
(Valium), digoxin (Lanoxin), erythro-
mycin (Erythrocin), furosemide (Lasix),
haloperidol (Haldol), hydrOXYzine
SIDE EFFECTS
(Vistaril), imipenem and cilastatin Occasional (4%–1%): Hypersensitivity
(Primaxin). reaction (chills, fever, pruritus, rash),
dizziness, drowsiness, headache, con-
stipation, diarrhea, nausea, vomiting,
IV COMPATIBILITIES abdominal pain.
Dexmedetomidine (Precedex), dilTIA-
Zem (Cardizem), DOBUTamine (Dobu- ADVERSE EFFECTS/TOXIC
trex), DOPamine (Intropin), heparin, REACTIONS
lipids, LORazepam (Ativan), midazolam
Exfoliative skin disorders, seri-
(Versed), propofol (Diprivan).
ous hepatic injury, blood dyscrasias
INDICATIONS/ROUTES/DOSAGE (eosinophilia, thrombocytopenia, ane-
mia, leukopenia) have been reported
b ALERT c PO and IV therapy equally
rarely. May increase risk of QT pro-
effective; IV therapy recommended for
longation, torsades de pointes. Skin
pts intolerant of drug or unable to take
disorders including Stevens-Johnson
orally. Oral suspension stable for 14
syndrome, toxic epidermal necrolysis
days at room temperature or refriger-
may occur.
ated.

underlined – top prescribed drug


fluorouracil, 5-FU 499

NURSING CONSIDERATIONS PRECAUTIONS


Contraindications: Hypersensitivity to flu-
BASELINE ASSESSMENT
orouracil. Myelosuppression, poor nutri-
Obtain CBC, LFT; serum potassium in crit- tional status, potentially serious infections.
ically ill pts. Receive full medication his- Cautions: History of high-dose pelvic irra-
tory and screen for interactions. Assess diation, hepatic/renal impairment, pal-
areas of infection. Assess infected area. mar-plantar erythrodysesthesia syndrome
INTERVENTION/EVALUATION (hand and foot syndrome), previous use
of alkylating agents. Pts with widespread
Assess for hypersensitivity reaction (chills, F
metastatic marrow involvement.
fever). Monitor CBC, BMP, LFT. Report
rash, itching promptly. Monitor tempera- ACTION
ture at least daily. Monitor daily pattern of
Blocks formation of thymidylic acid. Cell
bowel activity, stool consistency. Assess for
cycle–specific for S phase of cell division.
dizziness; provide assistance as needed.
Therapeutic Effect: Inhibits DNA, RNA
PATIENT/FAMILY TEACHING synthesis. Topical: Destroys rapidly pro-
• Report dark urine, pale stool, jaun- liferating cells.
diced skin or sclera of eyes, rash, pruri-
PHARMACOKINETICS
tus. • Pts with oropharyngeal infections
should maintain fastidious oral hy- Widely distributed. Crosses blood-brain bar-
giene. • Consult physician before tak- rier. Metabolized in liver. Primarily excreted
ing any other medication. by lungs as carbon dioxide. Removed by
hemodialysis. Half-life: 16 min.

LIFESPAN CONSIDERATIONS
fluorouracil, 5-FU Pregnancy/Lactation: If possible, avoid
use during pregnancy, esp. first trimes-
flure-oh-ue-ra-sil ter. May cause fetal harm. Unknown if
(Adrucil, Carac, Efudex, Fluoroplex, distributed in breast milk. Breastfeeding
Tolak) not recommended. Children: No age-
j BLACK BOX ALERT jMust be related precautions noted. Elderly: Age-
administered by personnel trained related renal impairment may require
in administration/handling of dosage adjustment.
chemotherapeutic agents.
Do not confuse Efudex with
Efidac. INTERACTIONS
DRUG: Bone marrow depressants
uCLASSIFICATION (e.g., cladribine) may increase risk of
PHARMACOTHERAPEUTIC: Antime- myelosuppression. Live virus vaccines
tabolite. CLINICAL: Antineoplastic. may potentiate virus replication, increase
vaccine side effects, decrease pt’s anti-
body response to vaccine. HERBAL: Echi-
USES nacea may decrease effects. FOOD: None
Parenteral: Treatment of carcinoma of known. LAB VALUES: May decrease
colon, rectum, breast, stomach (gastric), serum albumin. Topical: May cause
pancreas. Topical: Treatment of multiple eosinophilia, leukocytosis, thrombocyto-
actinic or solar keratoses, superficial basal penia, toxic granulation.
cell carcinomas. OFF-LABEL: Parenteral:
Treatment of carcinoma of bladder, cervi- AVAILABILITY (Rx)
cal, endometrial, head/neck, anal, esopha- Cream, Topical: (Carac): 0.5%. (Tolak): 4%,
geal, renal cell, unknown primary cancer. (Efudex): 5%. (Fluoroplex): 1%. Injection

Canadian trade name Non-Crushable Drug High Alert drug


500 fluorouracil, 5-FU
Solution: (Adrucil): 50 mg/mL. Solution, IV infusion: ADULTS, ELDERLY: 15 mg/kg/
Topical: (Efudex): 2%, 5%. day or 500 mg/m2/day over 4 hrs for 5 days
or 800–1200 mg/m2 over 24–120 hrs.
ADMINISTRATION/HANDLING
b ALERT c Give by IV injection or IV Multiple Actinic or Solar Keratoses
infusion. Do not add to other IV infu- Topical: (Carac 0.5%): ADULTS, ELDERLY:
sions. Avoid small veins, swollen/edema- Apply once daily for up to 4 wks. (Efudex
tous extremities, areas overlying joints, 5%): ADULTS, ELDERLY: Apply twice daily
tendons. May be carcinogenic, muta- for 2–4 wks. (Fluoroplex 1%): Apply
F genic, teratogenic. Handle with extreme twice daily for 2–6 wks. (Tolak 4%):
care during preparation/administration. Apply once daily for 4 wks.
IV Basal Cell Carcinoma
Topical: (Efudex 5%): ADULTS, ELDER­LY:
Reconstitution • IV push does not need Apply twice daily for 3–6 wks up to
to be diluted or reconstituted. • Inject 10–12 wks.
through Y-tube or 3-way stopcock of free-
flowing solution. • For IV infusion, further Dosage in Renal Impairment
dilute with 50–1,000 mL D5W or 0.9% NaCl. No dose adjustment.
Rate of administration • Give IV
push slowly over 1–2 min. • IV infu- Dosage in Hepatic Impairment
sion is administered over 30 min–24 hrs Use extreme caution.
(refer to individual protocols). • Ex-
travasation produces immediate pain, SIDE EFFECTS
severe local tissue damage. Parenteral: Frequent (greater than 10%):
Storage • Store at room tempera- Alopecia, dermatitis, anorexia, diarrhea,
ture. • Solution appears colorless to esophagitis, dyspepsia, stomatitis. Occa-
faint yellow. Slight discoloration does not sional (10%–1%): Cardiotoxicity (angina,
adversely affect potency or safety. • If ECG changes), skin dryness, epithelial
precipitate forms, redissolve by heating, fissuring, nausea, vomiting, excessive
shaking vigorously; allow to cool to body lacrimation, blurred vision. Rare (less
temperature. • Diluted solutions stable than 1%): Headache, photosensitivity,
for 72 hrs at room temperature. somnolence, allergic reaction, dyspnea,
hypotension, MI, pulmonary edema.
IV INCOMPATIBILITIES Topical: Occasional: Erythema, skin
Amphotericin B complex (Abelcet, AmBi- ulceration, pruritus, hyperpigmentation,
some, Amphotec), filgrastim (Neupo- dermatitis, insomnia, stomatitis, irritabil-
gen), ondansetron (Zofran), vinorelbine ity, photosensitivity, excessive lacrimation,
(Navelbine). blurred vision.
IV COMPATIBILITIES ADVERSE EFFECTS/TOXIC
Granisetron (Kytril), heparin, HYDROmor- REACTIONS
phone (Dilaudid), leucovorin, morphine, Earliest sign of toxicity (4–8 days after
potassium chloride, propofol (Diprivan). beginning therapy) is stomatitis (dry
mouth, burning sensation, mucosal
INDICATIONS/ROUTES/DOSAGE erythema, ulceration at inner margin
Note: Refer to individual protocols. of lips). Most common dermatologic
toxicity is pruritic rash (generally on
Usual Range extremities, less frequently on trunk).
IV bolus: ADULTS, ELDERLY:200–1000 Leukopenia (WBC less than 3500 cells/
mg/m2/day for 1–21 days or 500–600 mm3) generally occurs within 9–14
mg/m2/dose q3–4wks. days after drug administration but may
underlined – top prescribed drug
FLUoxetine 501
occur as late as 25th day. Thrombocyto- Proscar, or ProSom, or Sarafem
penia (platelets less than 100,000 cells/ with Serophene.
mm3) occasionally occurs within 7–17
days after administration. Pancytopenia, FIXED-COMBINATION(S)
agranulocytosis occur rarely. Symbyax: FLUoxetine/OLANZapine
(an antipsychotic): 25 mg/6 mg, 25
NURSING CONSIDERATIONS mg/12 mg, 50 mg/6 mg, 50 mg/12 mg.
BASELINE ASSESSMENT uCLASSIFICATION
Obtain baseline CBC with differential, se- PHARMACOTHERAPEUTIC: Selective F
rum renal function, LFT and monitor dur- serotonin reuptake inhibitor (SSRI).
ing therapy. Question history of hypersen- CLINICAL: Antidepressant.
sitivity reaction, hepatic/renal impairment.
INTERVENTION/EVALUATION
USES
Monitor for rapidly falling WBC, platelet
count; intractable diarrhea, GI bleeding Treatment of major depressive disorder
(bright red or tarry stool). Assess oral mu- (MDD), obsessive-compulsive disorder
cosa for stomatitis. Drug should be discon- (OCD), binge-eating and vomiting in
tinued if intractable diarrhea, stomatitis, GI moderate to severe bulimia nervosa, pre-
bleeding occurs. Assess skin for rash. menstrual dysphoric disorder (PMDD),
panic disorder with or without agora-
PATIENT/FAMILY TEACHING phobia. Treatment of resistant or bipo-
• Maintain strict oral hygiene. • Report lar 1 depression (with OLANZapine).
signs/symptoms of infection, unusual OFF-LABEL: Treatment of fibromyalgia,
bruising/bleeding, visual changes, nausea, post-traumatic stress disorder (PTSD),
vomiting, diarrhea, chest pain, palpita- Raynaud’s phenomena, social anxiety
tions. • Avoid sunlight, artificial light disorder, selective mutism.
sources; wear protective clothing, sun-
glasses, sunscreen. • Topical: Apply PRECAUTIONS
only to affected area. • Do not use oc- Contraindications: Hypersensitivity to
clusive coverings. • Be careful near eyes, FLUoxetine. Use of MAOIs within 5 wks of
nose, mouth. • Wash hands thoroughly discontinuing FLUoxetine or within 14 days
after application. • Treated areas may be of discontinuing MAOIs. Initiation in pts
unsightly for several weeks after therapy. receiving linezolid or methylene blue. Use
with pimozide or thioridazine. Note: Do
not initiate thioridazine until 5 wks after
discontinuing fluoxetine. Cautions: Seizure
FLUoxetine disorder, cardiac dysfunction (e.g., history
of MI), diabetes, pts with risk factors for QT
floo-ox-e-teen prolongation, concurrent use of medication
(PROzac, Sarafem) that increases QT interval, renal/hepatic
j BLACK BOX ALERT j Increased impairment, pts at high risk for suicide,
risk of suicidal thinking and in pts where weight loss is undesirable,
behavior in children, adolescents,
young adults 18–24 yrs of age with elderly. Pts at risk of acute narrow-angle
major depressive disorder, other glaucoma or with increased intraocular
psychiatric disorders. pressure.
Do not confuse FLUoxetine with
DULoxetine, famotidine, fluvas- ACTION
tatin, fluvoxaMINE, furosemide, Selectively inhibits serotonin uptake
or PARoxetine, or PROzac in CNS, enhancing serotonergic func-
with Paxil, PriLOSEC, Prograf, tion. Therapeutic Effect: Relieves
Canadian trade name Non-Crushable Drug High Alert drug
502 FLUoxetine
depression; reduces obsessive-compul- ADMINISTRATION/HANDLING
sive, bulimic behavior. PO
• Give without regard to food, but give with
PHARMACOKINETICS
food, milk if GI distress occurs. • Bipo-
Well absorbed from GI tract. Crosses lar disorder: Give once daily in eve-
blood-brain barrier. Protein binding: 94%. ning. • Depression, OCD: Give once
Metabolized in liver. Primarily excreted in daily in morning or twice daily (morning
urine. Not removed by hemodialysis. Half- and noon). • Bulimia: Give once daily in
life: 2–3 days; metabolite, 7–9 days. morning.
F
LIFESPAN CONSIDERATIONS INDICATIONS/ROUTES/DOSAGE
Pregnancy/Lactation: Unknown whe­ b ALERT c Use lower or less frequent
ther drug crosses placenta or is distributed doses in pts with renal/hepatic impair-
in breast milk. Children: May be more ment, pts with concurrent disease or
sensitive to behavioral side effects (e.g., multiple medications, the elderly. De-
insomnia, restlessness). Elderly: No age- crease gradually to minimize withdrawal
related precautions noted. symptoms and to allow for detection of
re-emerging symptoms.
INTERACTIONS
DRUG: NSAIDs (e.g., ibuprofen, ketor- Depression
olac, naproxen), antiplatelets (e.g., PO: ADULTS, ELDERLY: Initially, 20 mg
clopidogrel), anticoagulants (e.g., each morning. May increase after sev-
warfarin) may increase risk of bleed- eral wks by 20 mg/day. Maximum: 80
ing. Alcohol, other CNS depressants mg/day as single or 2 divided doses.
(e.g., LORazepam, morphine, zol- (Weekly): 90 mg/wk, begin 7 days after
pidem) may increase CNS depression. last dose of 20 mg in pts maintained on
MAOIs (e.g., phenelzine, selegiline) 20 mg/day. CHILDREN 8–18 YRS: Initially,
may produce serotonin syndrome and 10–20 mg/day. Lower-weight children may
neuroleptic malignant syndrome. Strong be started at 10 mg/day and increased to
CYP2D6 inhibitors (e.g., bupropion) 20 mg/day after several wks if needed.
may increase concentration/effect. May
decrease concentration/effect of tamoxi- Panic Disorder
fen. May enhance QT interval–prolong- PO: ADULTS, ELDERLY: Initially, 5–10
ing effects of thioridazine. May increase mg/day. After 3–7 days, may increase
adverse effects of tricyclic antidepres- dose in 5–10 mg increments at intervals
sants (e.g., amitriptyline). HERBAL: of at least 1 wk to usual dose of 20–40
Herbals with sedative properties mg/day. Maximum: 60 mg/day.
(e.g., chamomile, kava kava, vale-
rian) may increase CNS depression. St. Bulimia Nervosa
John’s wort may decrease concentra- PO: ADULTS: Initially, 20 mg/day. May
tion/effect. FOOD: None known. LAB VAL- increase by 20 mg increments at intervals
UES: May decrease serum sodium. May of at least 1 wk. Maximum: 60 mg/day.
increase serum ALT, AST. Obsessive-Compulsive Disorder (OCD)
AVAILABILITY (Rx) PO: ADULTS, ELDERLY: Initially, 10–20 mg
once daily. May increase by 20 mg incre-
Capsules: 10 mg, 20 mg, 40 mg. Oral
ments at intervals of at least 1 wk. Range:
Solution: 20 mg/5 mL. Tablets: 10 mg,
40–80 mg/day. Maximum: 80 mg/day.
20 mg, 60 mg. CHILDREN 7–18 YRS: Initially, 10 mg/day.
Capsules (Delayed-Release): 90 mg. May increase to 20 mg/day after 2 wks.
Range: 20–60 mg/day.

underlined – top prescribed drug


fluticasone 503
Depression Associated with Bipolar PATIENT/FAMILY TEACHING
Disorder • Maximum therapeutic response may
PO: ADULTS, ELDERLY, CHILDREN 10–17 YRS: require 4 or more wks of therapy. • Do
(With Olanzapine): Initially, 20 mg/day. not abruptly discontinue medica-
May increase gradually in 10–20 mg tion. • Avoid tasks that require alert-
increments. Range: 20–50 mg/day. ness, motor skills until response to drug
Premenstrual Dysphoric Disorder (PMDD) is established. • Avoid alcohol. • To
(Sarafem) avoid insomnia, take last dose of drug
PO: ADULTS: 20 mg/day continuously or before 4 PM.
F
20 mg/day beginning 14 days prior to men-
struation and continuing through first full
day of menses (repeated with each cycle).
fluticasone
Dosage in Renal/Hepatic Impairment
Use caution. floo-tik-a-sone
SIDE EFFECTS (Arnuity Ellipta, Cutivate, Flonase,
Flonase Allergy Relief, Flovent
Frequent (greater than 10%): Headache, Diskus, Xhance, Flonase Sensimist)
asthenia, insomnia, anxiety, drowsiness, Do not confuse Cutivate with Ul-
nausea, diarrhea, decreased appetite. Occa- travate, or Flonase with Flovent,
sional (9%–2%): Dizziness, tremor, fatigue, Beconase.
vomiting, constipation, dry mouth, abdomi-
nal pain, nasal congestion, diaphoresis, FIXED-COMBINATION(S)
rash. Rare (less than 2%): Flushed skin, Advair, Advair Diskus, Advair HFA:
light-headedness, impaired concentration. fluticasone/salmeterol (bronchodila-
ADVERSE EFFECTS/TOXIC tor): 100 mcg/50 mcg, 250 mcg/50
REACTIONS mcg, 500 mcg/50 mcg. Breo Ellipta:
May increase risk of suicide. Agitation, fluticasone/vilanterol (bronchodilator):
coma, diarrhea, delirium, hallucinations, 100 mcg/25 mcg. Dymista: flutica-
hyperreflexia, hyperthermia, tachycardia, sone/azelastine (an antihistamine): 50
seizures may indicate life-threatening mcg/137 mcg per spray. Trelegy El-
serotonin syndrome. lipta: fluticasone/umeclidinium (anti-
cholinergic)/vilanterol (bronchodila-
NURSING CONSIDERATIONS tor): 100 mcg/62.5 mcg/25 mcg.
BASELINE ASSESSMENT uCLASSIFICATION
Assess appearance, behavior, mood, sui- PHARMACOTHERAPEUTIC: Corticos-
cidal tendencies. For pts on long-term teroid. CLINICAL: Anti-inflammatory,
therapy, baseline renal function, LFT, blood antipruritic.
counts should be performed at baseline and
periodically thereafter.
USES
INTERVENTION/EVALUATION
Nasal: Management of nasal symptoms
Supervise suicidal-risk pt closely during
of perennial nonallergic rhinitis in adults
early therapy (as depression lessens, energy
and children 4 yrs and older. Manage-
level improves, increasing suicide poten-
ment of seasonal and perennial allergic
tial). Monitor mental status, anxiety, social
rhinitis in adults, children 2 yrs and
functioning, appetite, nutritional intake.
older. (Xhance): Treatment of nasal pol-
Monitor daily pattern of bowel activity, stool
yps in pts 18 yrs and older. (OTC): Relief
consistency. Assess skin for rash. Monitor
of hayfever/other upper respiratory aller-
serum LFT, glucose, sodium; weight.
gies. Topical: Relief of inflammation/
Canadian trade name Non-Crushable Drug High Alert drug
504 fluticasone
pruritus associated with steroid-respon- ritonavir) may increase concen-
sive disorders (e.g., contact dermatitis, tration/effect. HERBAL: Echinacea
eczema), atopic dermatitis. Inhalation: may decrease concentration/effects.
Maintenance treatment of bronchial FOOD: None known. LAB VALUES: None
asthma as prophylactic therapy. significant.
PRECAUTIONS AVAILABILITY (Rx)
Contraindications: Hypersensitivity to fluti- Aerosol for Oral Inhalation: (Flovent
casone. (Arnuity Ellipta, Flovent Diskus): HFA): 44 mcg/inhalation, 110 mcg/
F Severe hypersensitivity to milk proteins or inhalation, 220 mcg/inhalation.
lactose. Inhalation: Primary treatment Cream: (Cutivate): 0.05%. Ointment:
of status asthmaticus, acute exacerbation (Cutivate): 0.005%. Powder for Oral
of asthma, other acute asthmatic condi- Inhalation: (Flovent Diskus): 50 mcg/
tions. Cautions: Untreated systemic ocular blister, 100 mcg/blister, 250 mcg/
herpes simplex; untreated fungal, bacterial blister. (Arnuity Ellipta): 50 mcg/actua-
infection; active or quiescent tuberculosis. tion, 100 mcg/actuation, 200 mcg/
Thyroid disease, cardiovascular disease, actuation. Suspension Intranasal Spray:
diabetes, glaucoma, hepatic/renal impair- (Flonase Allergy Relief): 50 mcg/inha-
ment, cataracts, myasthenia gravis, seizures, lation. (Flonase Sensimist): 27.5 mcg/
GI disease, risk for osteoporosis, untreated spray. (Xhance): 93 mcg/actuation.
localized infection of nasal mucosa. Follow-
ing acute MI; concurrent use with strong ADMINISTRATION/HANDLING
CYP3A4 inhibitors. Inhalation
Flovent HFA
ACTION • Shake container well. Prime before
Direct local effect as potent vasoconstric- first use. Instruct pt to exhale com-
tor, anti-inflammatory. Therapeutic pletely. Place mouthpiece fully into
Effect: Prevents, controls inflammation. mouth, inhale, and hold breath as long
as possible before exhaling. • Allow
PHARMACOKINETICS 30–60 seconds between inhala-
Inhalation/intranasal: Protein bind- tions. • Rinsing mouth after each use
ing: 91%. Metabolized in liver. Excreted decreases dry mouth, hoarseness.
in urine. Half-life: 3–7.8 hrs. Topical: Flovent Diskus
Amount absorbed depends on affected • Do not shake or prime before use. Place
area and skin condition (absorption mouthpiece fully into mouth, inhale quickly
increased with fever, hydration, inflamed and deeply, remove device, and hold breath
or denuded skin). up to 10 seconds.
Arnuity Ellipta
LIFESPAN CONSIDERATIONS • Do not shake or prime before use;
Pregnancy/Lactation: Unknown if put mouthpiece between lips, breathe
drug crosses placenta or is distributed deeply and slowly through the mouth,
in breast milk. Children: Safety and effi- remove inhaler, and hold breath for 3–4
cacy not established in pts younger than 4 seconds.
yrs. Children 4 yrs and older may experi-
ence growth suppression with prolonged Intranasal
or high doses. Elderly: No age-related • Instruct pt to clear nasal passages as
precautions noted. much as possible before use (topical
nasal decongestants may be needed
INTERACTIONS 5–15 min before use). • Tilt head
DRUG: Strong CYP3A4 inhibitors slightly forward. • Insert spray tip into
(e.g., clarithromycin, ketoconazole, 1 nostril, pointing toward inflamed nasal

underlined – top prescribed drug


fluticasone 505
turbinates, away from nasal sep- 12 YRS AND OLDER: Initially, 100 mcg
tum. • Pump medication into 1 nostril twice daily. Maximum: 500 mcg twice
while pt holds other nostril closed, con- daily. (Flovent HFA): ADULTS, ELDERLY,
currently inspires through nose. CHILDREN 12 YRS AND OLDER: 88 mcg
twice daily. Maximum: 440 mcg twice
INDICATIONS/ROUTES/DOSAGE daily. USUAL PEDIATRIC DOSE (4–11 YRS):
Nonallergic Rhinitis (Flovent Diskus): Initially, 50 mcg
Intranasal: (Flonase): ADULTS, ELDERLY: twice daily. May increase to 100 mcg
Initially, 200 mcg (2 sprays in each nos- twice daily. (Flovent HFA): 88 mcg
tril once daily or 1 spray in each nostril twice daily. F
q12h). Maintenance: 1 spray in each
nostril once daily. May increase to 100 Dosage in Renal/Hepatic Impairment
mcg (2 sprays) in each nostril. Maxi- No dose adjustment. (Arnuity Ellipta):
mum: 200 mcg/day. CHILDREN 4 YRS AND Use caution in hepatic impairment.
OLDER: Initially, 100 mcg (1 spray in each
SIDE EFFECTS
nostril once daily). Maximum: 200
mcg/day (2 sprays each nostril). (Flo­ Frequent: Inhalation: Throat irrita-
nase Sensimist): ADULTS, ELDERLY, tion, hoarseness, dry mouth, cough,
CHILDREN 12 YRS AND OLDER: 110 mcg (2 temporary wheezing, oropharyngeal
sprays in each nostril) once daily. Main- candidiasis (particularly if mouth is not
tenance: 55 mcg (1 spray in each nos- rinsed with water after each administra-
tril) once daily. CHILDREN 2–11 YRS: 55 tion). Intranasal: Mild nasopharyngeal
mcg (1 spray in each nostril) once daily. irritation, nasal burning, stinging, dry-
ness, rebound congestion, rhinorrhea,
Allergic Rhinitis altered sense of taste. Occasional: Inha-
(Flonase Sensimist): ADULTS, ELDERLY, lation: Oral candidiasis. Intranasal:
CHILDREN 12 YRS AND OLDER: 110 mcg (2 Nasal/pharyngeal candidiasis, headache.
sprays in each nostril) once daily. Main- Topical: Stinging, burning of skin.
tenance: 55 mcg (1 spray in each nos-
tril) once daily. CHILDREN 2–11 YRS: 55 ADVERSE EFFECTS/TOXIC
mcg (1 spray in each nostril) once daily. REACTIONS
None known.
Usual Topical Dosage
Note: Ointment for adults only. NURSING CONSIDERATIONS
Topical: ADULTS, ELDERLY, CHILDREN BASELINE ASSESSMENT
3 MOS AND OLDER: Apply sparingly to Establish baseline history of skin disor-
affected area once or twice daily. der, asthma, rhinitis. Question hyper-
Nasal Polyps sensitivity, esp. milk products or lactose.
(Xhance): ADULTS, ELDERLY: 93 mcg Question medical history as listed in Pre-
(1 spray) per nostril twice daily. May cautions.
increase to 2 sprays twice daily. INTERVENTION/EVALUATION
Monitor rate, depth, rhythm, type of
Maintenance Treatment of Asthma respiration; quality/rate of pulse. As-
Inhalation powder: (Arnuity Ellipta): sess lung sounds for rhonchi, wheezing,
ADULTS, ELDERLY, CHILDREN 12 YRS AND rales. Assess oral mucous membranes
OLDER: 100–200 mcg once daily. for evidence of candidiasis. Monitor
Maximum: 200 mcg/day. CHILDREN growth in pediatric pts. Topical: Assess
5–11 YRS: 50 mcg once daily. (Flovent involved area for therapeutic response
Diskus): ADULTS, ELDERLY, CHILDREN to irritation.

Canadian trade name Non-Crushable Drug High Alert drug


506 fluvoxaMINE

PATIENT/FAMILY TEACHING Extended-Release: Treatment of OCD


in adults. OFF-LABEL: Treatment of social
• Pts receiving bronchodilators by inha- anxiety disorder (SAD), post-traumatic
lation concomitantly with steroid inhala- stress disorder (PTSD).
tion therapy should use bronchodilator
several min before corticosteroid aerosol PRECAUTIONS
(enhances penetration of steroid into Contraindications: Hypersensitivity to flu-
bronchial tree). • Do not change dose/ voxaMINE. Use of MAOIs concurrently or
schedule or stop taking drug; must taper within 14 days of discontinuing MAOIs or
F off gradually under medical supervi- fluvoxaMINE. Concomitant use with alos-
sion. • Maintain strict oral etron, pimozide, ramelteon, thioridazine,
hygiene. • Rinse mouth with water im- or tiZANidine. Initiation of fluvoxaMINE
mediately after inhalation (prevents in pts receiving linezolid or methylene
mouth/throat dryness, oral fungal infec- blue. Cautions: Renal/hepatic impair-
tion). • Increase fluid intake ment; elderly; impaired platelet aggrega-
(decreases lung secretion viscos- tion; concurrent use of NSAIDs, aspirin;
ity). • Intranasal: Clear nasal passages seizure disorder; pts that are volume
before use. • Report if no improvement depleted; third trimester of pregnancy; pts
in symptoms or if sneezing/nasal irrita- with high suicide risk; risk of bleeding or
tion occurs. • Improvement noted in receiving concurrent anticoagulant ther-
several days. • Topical: Rub thin film apy. May precipitate a shift to mania or
gently into affected area. • Use only for hypomania in pts with bipolar disorder.
prescribed area and no longer than or-
dered. • Avoid contact with eyes. ACTION
Selectively inhibits neuronal reuptake
of serotonin. Therapeutic Effect:
fluvoxaMINE Relieves depression, symptoms of obses-
sive-compulsive disorder (OCD).
floo-vox-a-meen PHARMACOKINETICS
(Luvox ) Well absorbed following PO admin-
j BLACK BOX ALERT jIncreased istration. Protein binding: 77%.
risk of suicidal ideation and behav­
ior in children, adolescents, young Metabolized in liver. Excreted in urine.
adults 18–24 yrs with major depres­ Half-life: 15–20 hrs.
sive disorder, other psychiatric
disorders. LIFESPAN CONSIDERATIONS
Do not confuse fluvoxaMINE Pregnancy/Lactation: Unknown if drug
with flavoxATE or FLUoxetine, crosses the placenta; distributed in breast
or Luvox with Lasix, Levoxyl, or milk. Children: Safety and efficacy not
Lovenox. established in pts younger than 8 yrs.
Elderly: Potential for reduced serum
uCLASSIFICATION
clearance; maintain caution.
PHARMACOTHERAPEUTIC: Selective
serotonin reuptake inhibitor. CLINI- INTERACTIONS
CAL: Antidepressant. DRUG: MAOIs (e.g., phenelzine, sele-
giline) may increase risk of serotonin
syndrome (hyperthermia, rigidity, myoclo-
USES nus). Tricyclic antidepressants (e.g.,
Immediate-Release: Treatment of amitriptyline) may increase concentra-
obsessive-compulsive disorder (OCD) tion/effect. Alcohol may increase adverse
in adults and children 8–17 yrs of age. effects. May increase concentration/effects

underlined – top prescribed drug


folic acid 507
of ramelteon, thioridazine, tiZANidine. ADVERSE EFFECTS/TOXIC
HERBAL: Herbals with anticoagulant/ REACTIONS
antiplatelet properties (e.g., garlic, Agitation, coma, diarrhea, delirium, hal-
ginger, ginkgo biloba), glucosamine lucinations, hyperreflexia, hyperthermia,
may increase effect. FOOD: Grapefruit tachycardia, seizures may indicate life-
products may increase concentration/ threatening serotonin syndrome.
effect. LAB VALUES: May decrease serum
sodium. NURSING CONSIDERATIONS
AVAILABILITY (Rx) BASELINE ASSESSMENT F
Tablets: 25 mg, 50 mg, 100 mg. Obtain LFT, BUN, serum creatinine; CrCl;
Capsules (Extended-Release): 100 urine/serum pregnancy test. Receive full
mg, 150 mg. medication history in screen for interac-
tions, esp. contraindicated use of con-
ADMINISTRATION/HANDLING comitant medications. Question history
• Do not break, crush, dissolve, or di- of seizure disorder. Assess hydration
vide extended-release capsules. • May status.
give with or without food. INTERVENTION/EVALUATION

INDICATIONS/ROUTES/DOSAGE Supervise suicidal-risk pt closely during


early therapy (as depression lessens,
Obsessive-Compulsive Disorder (OCD)
energy level improves, increasing sui-
PO: (Immediate-Release): ADULTS: Ini-
cide potential). Assess appearance, be-
tially, 50 mg at bedtime; may increase by 50 havior, speech pattern, level of interest,
mg every 4–7 days. Dosages greater than 100 mood. Assist with ambulation if dizziness,
mg/day should be given in 2 divided doses drowsiness occurs. Monitor daily pattern
with larger dose given at bedtime. Usual of bowel activity, stool consistency.
dose: 100–300 mg/day. Maximum: 300
mg/day. (Extended-Release): Initially, 100 PATIENT/FAMILY TEACHING
mg once daily at bedtime. May increase by • Maximum therapeutic response may
50 mg at no less than 1-wk intervals. Range: require 4 wks or more of therapy. • Dry
100–300 mg/day. Maximum: 300 mg/day. mouth may be relieved by sugarless gum,
CHILDREN 8–17 YRS: (Immediate-Release): sips of water. • Do not abruptly discon-
Initially, 25 mg at bedtime; may increase tinue medication. • Avoid tasks that
by 25 mg every 4–7 days. Dosages greater require alertness, motor skills until re-
than 50 mg/day should be given in 2 divided sponse to drug is established.
doses with larger dose given at bedtime.
Maximum: (CHILDREN 8–11 YRS): 200 mg/
day. (CHILDREN 12–17 YRS): 300 mg/day.
folic acid
Dosage in Renal/Hepatic Impairment
No dose adjustment. foe-lik as-id
(Apo-Folic )
SIDE EFFECTS Do not confuse folic acid with
Frequent (40%–21%): Nausea, head- folinic acid.
ache, drowsiness, insomnia. Occasional
(14%–8%): Dizziness, diarrhea, dry mouth, uCLASSIFICATION
asthenia, dyspepsia, constipation, abnor- PHARMACOTHERAPEUTIC: Vitamin,
mal ejaculation. Rare (6%–3%): Anorexia, water soluble. CLINICAL: Nutritional
anxiety, tremor, vomiting, flatulence, urinary supplement.
frequency, sexual dysfunction, altered taste.

Canadian trade name Non-Crushable Drug High Alert drug


508 folic acid

USES IV
Treatment of megaloblastic and macrocytic
anemias due to folate deficiency. Treat- May give 5 mg or less undiluted over at
ment of anemias due to folate deficiency in least 1 min, or dilute with 50 mL 0.9%
pregnant women. Folate supplementation NaCl or D5W and infuse over 30 min.
during periconceptual period decreases INDICATIONS/ROUTES/DOSAGE
risk of neural tube defects.
Anemia
PRECAUTIONS IM/IV/SQ/PO: ADULTS, ELDERLY, CHIL-
F Contraindications: Hypersensitivity to DREN 4 YRS AND OLDER: 1–5 mg/day.
folic acid. Cautions: Anemias (aplas- CHILDREN YOUNGER THAN 4 YRS: Up to
tic, normocytic, pernicious, refractory) 0.3 mg/day. INFANTS: 0.1 mg/day. PREG-
when anemia present with vitamin B12 NANT/LACTATING WOMEN: 0.8 mg/day.
deficiency. Prevention of Neural Tube Defects
ACTION PO: WOMEN OF CHILDBEARING AGE:
400–800 mcg/day. WOMEN AT HIGH
Stimulates production of platelets, WBCs RISK OR FAMILY HISTORY OF NEURAL TUBE
in folate-deficiency anemia. Necessary for DEFECTS: 4 mg/day.
formation of co-enzymes in many meta-
bolic pathways. Necessary for erythropoi- SIDE EFFECTS
esis. Therapeutic Effect: Essential for None known.
nucleoprotein synthesis, maintenance of
normal erythropoiesis. ADVERSE EFFECTS/TOXIC
REACTIONS
PHARMACOKINETICS
Allergic hypersensitivity occurs rarely
PO form almost completely absorbed with parenteral form. Oral folic acid is
from GI tract (upper duodenum). nontoxic.
Protein binding: High. Metabolized in
liver. Excreted in urine. Removed by NURSING CONSIDERATIONS
hemodialysis.
BASELINE ASSESSMENT
LIFESPAN CONSIDERATIONS Pernicious anemia should be ruled out
Pregnancy/Lactation: Distributed in with Schilling test and vitamin B12 blood
breast milk. Children/Elderly: No age- level before initiating therapy (may pro-
related precautions noted. duce irreversible neurologic damage).
Resistance to treatment may occur if de-
INTERACTIONS creased hematopoiesis, alcoholism, anti-
DRUG: None significant. HERBAL: Green metabolic drugs, deficiency of vitamin B6,
tea may increase concentration. B12, C, E is evident.
FOOD: None known. LAB VALUES: May
INTERVENTION/EVALUATION
decrease vitamin B12 concentration.
Assess for therapeutic improvement: im-
AVAILABILITY (Rx) proved sense of well-being, relief from
Capsules: 0.8 mg, 5 mg, 20 mg. Injec- iron deficiency symptoms (fatigue, short-
tion Solution: 5 mg/mL. Tablets: 0.4 mg ness of breath, sore tongue, headache,
(OTC), 0.8 mg (OTC), 1 mg. pallor).
PATIENT/FAMILY TEACHING
ADMINISTRATION/HANDLING
PO
• Eat foods rich in folic acid, including
• May give without regard to food. fruits, vegetables, organ meats.

underlined – top prescribed drug


fondaparinux 509
stopping blood coagulation cascade.
fondaparinux Therapeutic Effect: Indirectly pre-
vents formation of thrombin and subse-
fon-dap-a-rin-ux quently fibrin clot.
(Arixtra)
j BLACK BOX ALERT jEpidural PHARMACOKINETICS
or spinal anesthesia greatly in­ Well absorbed after SQ administration.
creases potential for spinal or
epidural hematoma, subsequent Undergoes minimal, if any, metabo-
long-term or permanent paralysis. lism. Highly bound to antithrombin
III. Distributed mainly in blood and to F
uCLASSIFICATION a minor extent in extravascular fluid.
PHARMACOTHERAPEUTIC: Factor Xa Excreted unchanged in urine. Removed
inhibitor. CLINICAL: Antithrombotic. by hemodialysis. Half-life: 17–21 hrs
(increased in renal impairment).

USES LIFESPAN CONSIDERATIONS


Prevention of venous thromboembolism Pregnancy/Lactation: Use with cau-
in pts undergoing total hip replacement, tion, particularly during third trimester,
hip fracture surgery, knee replacement immediate postpartum period (increased
surgery, abdominal surgery. Treatment of risk of maternal hemorrhage). Unknown
acute deep vein thrombosis (DVT), acute if excreted in breast milk. Chil-
pulmonary embolism in conjunction with dren: Safety and efficacy not established.
warfarin. OFF-LABEL: Prophylaxis of DVT Elderly: Age-related renal impairment
in pts with history of heparin-induced may increase risk of bleeding.
thrombocytopenia (HIT), acute symptom-
atic superficial vein thrombosis of the legs. INTERACTIONS
DRUG: Anticoagulants (e.g., hepa-
PRECAUTIONS rin, warfarin), aspirin, NSAIDs (e.g.,
Contraindications: Hypersensitivity to fond­ ibuprofen, ketorolac, naproxen)
aparinux, active major bleeding, bacterial may increase risk of bleeding. May
endocarditis, prophylaxis treatment in pts increase effect of apixaban, dabi-
with body weight less than 50 kg, severe gatran, edoxaban, rivaroxaban.
renal impairment (CrCl less than 30 mL/ HERBAL: Herbals with anticoagulant/
min), thrombocytopenia associated with antiplatelet properties (e.g., garlic,
antiplatelet antibody formation in presence ginger, ginkgo biloba) may increase
of fondaparinux. Cautions: Conditions effect. FOOD: None known. LAB VAL-
with increased risk of bleeding, bacterial UES: May cause reversible increases in
endocarditis, active ulcerative GI disease, serum creatinine, ALT, AST. May decrease
hemorrhagic stroke; shortly after brain, Hgb, Hct, platelet count.
spinal, or ophthalmologic surgery; concur-
rent platelet inhibitors, severe uncontrolled AVAILABILITY (Rx)
hypertension, history of CVA, history of 2.5 mg/0.5 mL, 5
Injection, Solution:
heparin-induced thrombocytopenia, renal/ mg/0.4 mL, 7.5 mg/0.6 mL, 10 mg/0.8 mL.
hepatic impairment, elderly, indwelling epi-
dural catheter use. ADMINISTRATION/HANDLING
SQ
ACTION • Parenteral form appears clear, color-
Factor Xa inhibitor that selectively binds less. Discard if discoloration or particulate
to antithrombin and increases its affin- matter is noted. • Store at room tempera-
ity for factor Xa, inhibiting factor Xa, ture. • Do not expel air bubble from

Canadian trade name Non-Crushable Drug High Alert drug


510 fondaparinux
prefilled syringe before injection. • Insert Rare (less than 4%): Dizziness, hypoten-
needle subcutaneously into upper arm, sion, confusion, urinary retention, injec-
outer thigh, or abdomen and inject solu- tion site hematoma, diarrhea, dyspepsia,
tion. • Do not inject into areas of active headache.
skin disease or injury such as sunburns,
rashes, inflammation, skin infections, ADVERSE EFFECTS/TOXIC
or active psoriasis. • Rotate injection REACTIONS
sites. Accidental overdose may lead to bleeding
complications ranging from local ecchy-
F INDICATIONS/ROUTES/DOSAGE moses to major hemorrhage. Thrombo-
b ALERT c For SQ administration only. cytopenia occurs rarely.
Prevention of Venous Thromboembolism NURSING CONSIDERATIONS
SQ: ADULTS WEIGHING 50 KG OR MORE: 2.5
BASELINE ASSESSMENT
mg once daily for 5–9 days after surgery (up
to 10 days following abdominal surgery; 11 Assess CBC, renal function test. Evalu-
days following hip or knee replacement). ate potential risk for bleeding. Ques-
Initial dose should be given no earlier than tion history of recent surgery, trauma,
6–8 hrs after surgery. Initiate dose once intracranial hemorrhage, GI bleed-
hemostasis established. WEIGHING LESS ing. Question medical history as listed
THAN 50 KG: Contraindicated. in Precautions. Ensure that pt has not
received spinal anesthesia, spinal pro-
Treatment of Venous Thromboembolism, cedures.
Pulmonary Embolism
INTERVENTION/EVALUATION
Note: Start warfarin on first treatment
day and continue fondaparinux until INR Periodically monitor CBC, esp. platelet
reaches 2 to 3 for at least 24 hr. Usual count, stool for occult blood (no need
duration of fondaparinux: 5–9 days. for daily monitoring in pts with normal
SQ: ADULTS, ELDERLY WEIGHING MORE presurgical coagulation parameters).
THAN 100 KG: 10 mg once daily. ADULTS, Assess for any signs of bleeding: bleed-
ELDERLY WEIGHING 50–100 KG: 7.5 mg ing at surgical site, hematuria, blood in
once daily. ADULTS, ELDERLY WEIGHING stool, bleeding from gums, petechiae,
LESS THAN 50 KG: 5 mg once daily. ecchymosis, bleeding from injection
sites. Monitor B/P, pulse; hypotension,
Dosage in Renal Impairment tachycardia may indicate bleeding, hypo-
CrCl greater than 50 mL/min: No dose volemia.
adjustment. CrCl 30–50 mL/min: Use
PATIENT/FAMILY TEACHING
caution (50% dose reduction or use of
low-dose heparin). CrCl less than 30 • Usual length of therapy is 5–9
mL/min: Contraindicated. days. • Do not take any OTC medica-
tion (esp. aspirin, NSAIDs). • Report
Dosage in Hepatic Impairment swelling of hands/feet, unusual back
Mild to moderate impairment: No dose pain, unusual bleeding/bruising, weak-
adjustment. Severe impairment: Use ness. Treatment may increase risk of
caution. bleeding into the brain; report confu-
sion, one-sided weakness, trouble
SIDE EFFECTS speaking, seizures. Treatment may in-
Frequent (19%–11%): Anemia, fever, crease risk of GI bleeding; report
nausea. Occasional (10%–4%): Edema, bloody stool, vomiting up blood; dark,
constipation, rash, vomiting, insomnia, tarry stools.
increased wound drainage, hypokalemia.

underlined – top prescribed drug


fosinopril 511
Slowly absorbed from GI tract. Protein
fosinopril binding: 97%–98%. Metabolized in liver
and GI mucosa. Primarily excreted in
foe-sin-oh-pril urine. Minimal removal by hemodialysis.
j BLACK BOX ALERT jMay Half-life: 11.5 hrs.
cause fetal injury, mortality. Dis­
continue as soon as possible once LIFESPAN CONSIDERATIONS
pregnancy is detected.
Do not confuse fosinopril with Pregnancy/Lactation: Crosses pla-
Fosamax or lisinopril, or Mono- centa. Distributed in breast milk. May
pril with Accupril, minoxidil, cause fetal or neonatal mortality or mor- F
moexipril, or ramipril. bidity. Children: Safety and efficacy not
established. Neonates, infants may be at
uCLASSIFICATION increased risk for oliguria, neurologic
PHARMACOTHERAPEUTIC: ACE in- abnormalities. Elderly: May be more
hibitor. CLINICAL: Antihypertensive. sensitive to hypotensive effects.
INTERACTIONS
USES DRUG: Potassium-sparing diuretics
Treatment of hypertension. Adjunctive (e.g., spironolactone), potassium
treatment of HF. supplements may cause hyperkalemia.
May increase lithium concentration/tox-
PRECAUTIONS icity. Antacids may decrease absorption.
Contraindications: Hypersensitivity to Aliskiren may increase hyperkalemic
fosinopril. History of angioedema from effect. May increase potential for allergic
previous treatment with ACE inhibitors. reactions to allopurinol. Angiotensin
Concomitant use with aliskiren in pts receptor blockers (ARBs)(e.g., losar-
with diabetes. Cautions: Renal/hepatic tan, valsartan) may increase adverse
impairment, pts with sodium depletion effects. May increase adverse effects of lith-
or on diuretic therapy, dialysis, hypovo- ium, sacubitril. HERBAL: Herbals with
lemia, hypertrophic cardiomyopathy with hypertensive properties (e.g., licorice,
outflow tract obstruction, hyperkalemia, yohimbe) or hypotensive properties
concomitant use of potassium supple- (e.g., garlic, ginger, ginkgo biloba)
ments, unstented unilateral/bilateral may alter effects. FOOD: None known.
renal stenosis, diabetes, severe aortic LAB VALUES: May increase serum BUN,
stenosis. Before, during, or immediately alkaline phosphatase, bilirubin, creatinine,
after major surgery. potassium, ALT, AST. May decrease serum
sodium. May cause positive antinuclear an-
ACTION tibody titer (ANA).
Suppresses renin-angiotensin-aldo­s­terone
system (prevents conversion of angioten- AVAILABILITY (Rx)
sin I to angiotensin II, a potent vasocon- Tablets: 10 mg, 20 mg, 40 mg.
strictor; may inhibit angiotensin II at local
vascular, renal sites). Decreases plasma ADMINISTRATION/HANDLING
angiotensin II, increases plasma renin PO
activity, decreases aldosterone secretion. • Give without regard to food. • Tab-
Therapeutic Effect: Reduces B/P. lets may be crushed.
PHARMACOKINETICS INDICATIONS/ROUTES/DOSAGE
Route Onset Peak Duration Hypertension
PO 1 hr 2–6 hrs 24 hrs PO: ADULTS, ELDERLY:Initially, 10 mg
once daily. Maintenance: 10–40 mg
Canadian trade name Non-Crushable Drug High Alert drug
512 fosphenytoin
once daily. Maximum: 80 mg once daily. INTERVENTION/EVALUATION
CHILDREN 6–16 YRS WEIGHING MORE THAN If excessive reduction in B/P occurs,
50 KG: Initially, 5–10 mg once daily. Maxi- place pt in supine position with legs el-
mum: 40 mg once daily. WEIGHING 50 KG evated. Assist with ambulation if dizziness
OR LESS: Initially, 0.1 mg/kg once daily. May occurs. Assess for urinary frequency.
increase up to a maximum of 0.6 mg/kg not Auscultate lung sounds for rales, wheez-
to exceed 40 mg/day. ing in pts with HF. Monitor renal function
HF
tests, CBC, urinalysis for proteinuria. Ob-
PO: ADULTS, ELDERLY: Initially, 10 mg serve for angioedema (swelling of face,
F lips, tongue). Monitor serum potassium
once daily. May increase dose over sev-
eral wks. Maintenance: 20–40 mg in those on concurrent diuretic therapy.
once daily. Maximum: 40 mg once daily. PATIENT/FAMILY TEACHING
Dosage in Renal Impairment • Report any sign of infection (sore
Reduce initial dose to 5 mg in pts with HF. throat, fever). • Several wks may be
needed for full therapeutic effect of B/P
Dosage in Hepatic Impairment
reduction. • Skipping doses or volun-
No dose adjustment. tarily discontinuing drug may produce
SIDE EFFECTS severe rebound hypertension. • To re-
Frequent (12%–9%): Dizziness, cough. Occa­ duce hypotensive effect, go from lying to
sional (4%–2%): Hypotension, nausea, vom- standing slowly. • Immediately report
iting, upper respiratory tract infection. swelling of face, lips, tongue, difficulty
breathing, vomiting, excessive perspira-
ADVERSE EFFECTS/TOXIC tion, persistent cough. • Avoid potas-
REACTIONS sium salt substitutes.
Excessive hypotension (“first-dose syn-
cope”) may occur in pts with HF, severely
salt/volume depleted. Angioedema (swell-
ing of face/lips), hyperkalemia occur fosphenytoin
rarely. Agranulocytosis, neutropenia may
be noted in pts with renal impairment, fos-fen-i-toyn
collagen vascular disease (scleroderma, (Cerebyx)
systemic lupus erythematosus). Nephrotic Do not confuse Cerebyx with
syndrome may be noted in those with his- CeleBREX or CeleXA, or fosphe-
tory of renal disease. nytoin with fospropofol.

NURSING CONSIDERATIONS uCLASSIFICATION


PHARMACOTHERAPEUTIC: Hydan-
BASELINE ASSESSMENT
toin. CLINICAL: Anticonvulsant.
Obtain B/P immediately before each dose,
in addition to regular monitoring (be alert
to fluctuations). Renal function tests should USES
be performed before beginning therapy. In Control of generalized tonic-clonic status
pts with renal impairment, autoimmune epilepticus convulsive status epilepticus.
disease, or taking drugs that affect leuko- Prevention, treatment of seizures occur-
cytes or immune response, CBC, differential ring during neurosurgery. Short-term
count should be performed before therapy substitution for oral phenytoin.
begins and q2wks for 3 mos, then periodi-
cally thereafter. Question medical history as PRECAUTIONS
listed in Precautions. Question history of Contraindications: Hypersensitivity to
hypersensitivity reaction, angioedema. fosph­enytoin, phenytoin, other hydantoins.

underlined – top prescribed drug


fosphenytoin 513
Adams-Stokes syndrome; second- or ADMINISTRATION/HANDLING
third-degree AV block; sinus bradycardia;
IV
SA block; concurrent use of delavirdine.
History of hepatotoxicity attributed to Reconstitution • Dilute in D5W or
fosphenytoin or phenytoin. Cautions: Por- 0.9% NaCl to a concentration ranging
phyria, diabetes, hypothyroidism, hypo- from 1.5–25 mg PE/mL.
tension, severe myocardial insufficiency, Rate of administration • Administer
renal/hepatic disease, hypoalbuminemia. at rate less than 150 mg PE/min (de-
creases risk of hypotension, arrhyth-
ACTION mias). Children: 2 mg PE/kg/min. Maxi- F
Stabilizes neuronal membranes, limits mum: 150 mg PE/min.
spread of seizure activity by increasing Storage • Refrigerate. • Do not
efflux or decreasing influx of sodium ions store at room temperature for longer
across cell membranes in the motor cortex than 48 hrs. • After dilution, solution is
during nerve impulse generation. Thera- stable for 8 hrs at room temperature or
peutic Effect: Decreases seizure activity. 24 hrs if refrigerated.
PHARMACOKINETICS IV INCOMPATIBILITIES
Completely absorbed after IM administra- Midazolam (Versed).
tion. Protein binding: 95%–99%. Rapidly
and completely hydrolyzed to phenytoin IV COMPATIBILITIES
after IM or IV administration. Time of LORazepam (Ativan), PHENobarbital,
complete conversion to phenytoin: 4 hrs potassium chloride.
after IM injection; 2 hrs after IV infusion.
Half-life: 8–15 min (for conversion to INDICATIONS/ROUTES/DOSAGE
phenytoin). (Phenytoin: 12–29 hrs.) b ALERT c 150 mg fosphenytoin yields
100 mg phenytoin. Dosage, concentration
LIFESPAN CONSIDERATIONS
solution, infusion rate of fosphenytoin are
Pregnancy/Lactation: May increase expressed in terms of phenytoin equivalents
frequency of seizures during pregnancy. (PE).
Increased risk of congenital malformations.
Unknown if excreted in breast milk. Chil- Status Epilepticus
dren: Safety and efficacy not established. IV: ADULTS: Loading dose: 20 mg PE/
Elderly: Lower dosage recommended. kg infused at rate of 100–150 mg PE/
min. May give an additional 5–10 mg
INTERACTIONS PE/kg 10 min after loading dose. Maxi-
DRUG: Alcohol, other CNS depressants mum total loading dose: 30 mg PE/kg.
(e.g., LORazepam, morphine, zol- Maintenance dose: Initially, 4–7 mg PE/
pidem) may increase CNS depression. May kg/day (usual daily dose: 300–400 mg
decrease concentration/effect of apixaban, PE) given in 2–4 divided doses.
axitinib, dabigatran, dronedarone,
itraconazole, ivabradine, nimodipine, Nonemergent Seizures
rivaroxaban. HERBAL: Herbals with IV, IM: ADULTS: Loading dose: 10–
sedative properties (e.g., chamomile, 20 mg PE/kg. Maintenance: 4–6 mg
kava kava, valerian) may increase CNS PE/kg/day in divided doses.
depression. FOOD: None known. LAB VAL-
UES: May increase serum glucose, GGT, Short-Term Substitution for Oral Phenytoin
alkaline phosphatase. IV, IM: ADULTS: May substitute for oral
phenytoin at same total daily dose.
AVAILABILITY (Rx)
Injection Solution: 100 mg PE/2 mL, 500 Dosage in Renal/Hepatic Impairment
mg PE/10 mL. No dose adjustment.
Canadian trade name Non-Crushable Drug High Alert drug
514 frovatriptan

SIDE EFFECTS USES


Frequent: Dizziness, paresthesia, tin- Acute treatment of migraine headache
nitus, pruritus, headache, drowsiness. with or without aura in adults.
Occasional: Morbilliform rash.
PRECAUTIONS
ADVERSE EFFECTS/TOXIC
REACTIONS Contraindications: Hypersensitivity to
frovatriptan. Management of basilar or
Toxic fosphenytoin serum concentration hemiplegic migraine, cerebrovascular
may produce ataxia (muscular incoor- or peripheral vascular disease, coronary
F dination), nystagmus (rhythmic oscilla- artery disease, ischemic heart disease
tion of eyes), diplopia, lethargy, slurred (angina pectoris, history of MI, silent
speech, nausea, vomiting, hypotension. ischemia, Prinzmetal’s angina), severe
As drug level increases, extreme lethargy hepatic impairment (Child-Pugh Grade
may progress to coma. C), uncontrolled hypertension, use
NURSING CONSIDERATIONS within 24 hrs of ergotamine-containing
preparations or another serotonin recep-
BASELINE ASSESSMENT tor agonist. Cautions: Mild to moderate
Review history of seizure disorder (in- hepatic impairment, pt profile suggesting
tensity, frequency, duration, LOC). Initiate cardiovascular risks. History of seizures
seizure precautions. Obtain vital signs, or structural brain lesions.
medication history (esp. use of phenytoin,
other anticonvulsants). Observe clinically. ACTION
Selective agonist for serotonin in cranial
INTERVENTION/EVALUATION
arteries causing vasoconstriction and
Monitor ECG, measure cardiac function, reduction of inflammation. Therapeutic
respiratory function, B/P during and im- Effect: Relieves migraine headache.
mediately following infusion (10–20 min).
Discontinue if skin rash appears. Interrupt PHARMACOKINETICS
or decrease rate if hypotension, arrhyth- Well absorbed after PO administra-
mias are detected. Assess pt postinfusion tion. Protein binding: 15%. Metabolized
(may feel dizzy, ataxic, drowsy). Monitor in liver. Primarily eliminated in feces
free and total dilantin levels (2 hrs after IV (62%), urine (32%). Half-life: 26 hrs
infusion or 4 hrs after IM injection). (increased in hepatic impairment).
PATIENT/FAMILY TEACHING
LIFESPAN CONSIDERATIONS
• If noncompliance is cause of acute
seizures, discuss and address reasons for Pregnancy/Lactation: Unknown if drug
noncompliance. • Avoid tasks that re- is excreted in breast milk. Children: Safety
quire alertness, motor skills until re- and efficacy not established. Elderly: Not
sponse to drug is established. recommended for use in this pt population.
INTERACTIONS
frovatriptan DRUG: Ergotamine-containing medi-
cations may produce vasospastic reaction.
froe-va-trip-tan May increase adverse effect of SUMAtrip-
(Frova) tan. Antiemetics (5-HT3 antagonists),
antiparkinson agents (MAOIs),
uCLASSIFICATION linezolid, metOLazone, opioid ago-
PHARMACOTHERAPEUTIC: Seroto- nists may increase serotonergic effect.
nin 5-HT1 receptor agonist. CLINI- HERBAL: None significant. FOOD: None
CAL: Antimigraine. known. LAB VALUES: None significant.

underlined – top prescribed drug


furosemide 515

AVAILABILITY (Rx) INTERVENTION/EVALUATION

Tablets: 2.5 mg. Assess for relief of migraine headache,


potential for photophobia, phonophobia
ADMINISTRATION/HANDLING (sound sensitivity), nausea, vomiting.
PO PATIENT/FAMILY TEACHING
• Give with fluids as soon as symptoms • Take a single dose as soon as symp-
appear. • Do not break, crush, dis- toms of an actual migraine attack ap-
solve, or divide film-coated tablets. pear. • Medication is intended to re-
INDICATIONS/ROUTES/DOSAGE lieve migraine headaches, not to prevent F
or reduce number of attacks. • Avoid
Acute Migraine Headache tasks that require alertness, motor skills
PO: ADULTS, ELDERLY: Initially, 2.5 mg. until response to drug is estab-
If headache improves but then returns, lished. • Immediately report palpita-
dose may be repeated after at least 2 hrs. tions, pain, tightness in chest or throat,
Maximum: 7.5 mg/day. sudden or severe abdominal pain, pain
Dosage in Renal Impairment
or weakness of extremities.
No dose adjustment.
Dosage in Hepatic Impairment
Mild to moderate impairment: No
furosemide
dose adjustment. Severe impairment:
fur-oh-se-myde
Use caution.
(Apo-Furosemide , Lasix)
SIDE EFFECTS j BLACK BOX ALERT jLarge
doses can lead to profound diuresis
Occasional (8%–4%): Dizziness, paresthe­ with water and electrolyte deple­
sia, fatigue, flushing. Rare (3%–2%): tion.
Hot/cold sensation, dry mouth, Do not confuse furosemide with
dyspepsia. famotidine, finasteride, flucona-
zole, FLUoxetine, loperamide,
ADVERSE EFFECTS/TOXIC or torsemide, or Lasix with
REACTIONS Lidex, Lovenox, Luvox, or Luxiq.
Cardiac reactions (ischemia, coronary
artery vasospasm, MI), noncardiac uCLASSIFICATION
vasospasm-related reactions (cerebral PHARMACOTHERAPEUTIC: Loop
hemorrhage, CVA) occur rarely, partic- diuretic. CLINICAL: Diuretic. Antihy-
ularly in pts with hypertension, obesity, pertensive.
smokers, diabetes, strong family his-
tory of coronary artery disease; males
older than 40 yrs; postmenopausal USES
women. Treatment of edema associated with
HF and renal/hepatic disease; acute
NURSING CONSIDERATIONS pulmonary edema. Treatment of hyper-
BASELINE ASSESSMENT tension (not recommended as initial
treatment).
Question for history of peripheral
vascular disease, renal/hepatic im- PRECAUTIONS
pairment, possibility of pregnancy.
Contraindications: Hypersensitivity to
Question regarding onset, location,
furosemide. Anuria. Cautions: Hepatic
duration of migraine, possible precipi-
cirrhosis, hepatic coma, severe elec-
tating factors.
trolyte depletion, prediabetes, diabetes,
Canadian trade name Non-Crushable Drug High Alert drug
516 furosemide
systemic lupus erythematosus. Pts with (e.g., garlic, ginger, ginkgo biloba)
prostatic hyperplasia/urinary stricture. may alter effects. FOOD: None known.
LAB VALUES: May increase serum glu-
ACTION cose, BUN, uric acid. May decrease
Inhibits reabsorption of sodium, chloride serum calcium, chloride, magnesium,
in ascending loop of Henle and proxi- potassium, sodium.
mal/distal renal tubules. Therapeutic
Effect: Increases excretion of water, AVAILABILITY (Rx)
sodium, chloride, magnesium, calcium. Injection Solution: 10 mg/mL. Solu-
F tion, Intravenous: 100 mg/100 mL. Oral
PHARMACOKINETICS Solution: 10 mg/mL, 40 mg/5 mL. Tab-
Route Onset Peak Duration lets: 20 mg, 40 mg, 80 mg.
PO 30–60 min 1–2 hrs 6–8 hrs
IV 5 min 20–60 min 2 hrs ADMINISTRATION/HANDLING
IM 30 min N/A N/A
IV
Moderately absorbed from GI tract. Protein
binding: greater than 98%. Partially metab- Rate of administration • May give
olized in liver. Primarily excreted in urine undiluted but is compatible with D5W or
(nonrenal clearance increases in severe 0.9% NaCl. • May be diluted for infu-
renal impairment). Not removed by hemo- sion to 1–2 mg/mL (Maximum: 10 mg/
dialysis. Half-life: 30–90 min (increased mL). • Administer each 40 mg or frac-
in renal/hepatic impairment, neonates). tion by IV push over 1–2 min. Do not
exceed administration rate of 4 mg/min
LIFESPAN CONSIDERATIONS for short-term intermittent infusion.
Pregnancy/Lactation: Crosses placenta. Storage • Solution appears clear, color-
Distributed in breast milk. Children: Half- less. • Discard yellow solutions. • Sta-
life increased in neonates; may require ble for 24 hrs at room temperature when
increased dosage interval. Elderly: May mixed with 0.9% NaCl or D5W.
be more sensitive to hypotensive, electro- IM
lyte effects, developing circulatory collapse, • Temporary pain at injection site may
thromboembolic effect. Age-related renal be noted.
impairment may require dosage adjustment.
PO
INTERACTIONS • Administer on empty stom-
DRUG: Bile acid sequestrants (e.g., ach. • Give with food to avoid GI upset,
cholestyramine), sucralfate may preferably with breakfast (may prevent
decrease absorption/effect. May increase nocturia). • Food may decrease di-
hyponatremic effect of desmopressin. uretic effect.
May increase QT interval–prolonging
effect of dofetilide. Amphotericin B, IV INCOMPATIBILITIES
nephrotoxic ototoxic medications Ciprofloxacin (Cipro), dilTIAZem
(e.g., lisinopril, IV contrast dye, (Cardizem), DOBUTamine (Dobutrex),
vancomycin) may increase risk of neph- DOPamine (Intropin), DOXOrubicin
rotoxicity, ototoxicity. May increase risk (Adriamycin), droperidol (Inapsine),
of lithium toxicity. Other medications esmolol (Brevibloc), famotidine (Pepcid),
causing hypokalemia (e.g., HCTZ, filgrastim (Neupogen), fluconazole (Diflu-
laxatives) may increase risk of hypoka- can), gemcitabine (Gemzar), gentamicin
lemia. HERBAL: Herbals with hyper- (Garamycin), IDArubicin (Idamycin),
tensive properties (e.g., licorice, labetalol (Trandate), metoclopramide
yohimbe) or hypotensive properties (Reglan), midazolam (Versed), milrinone

underlined – top prescribed drug


furosemide 517
(Primacor), niCARdipine (Cardene), Dosage in Hepatic Impairment
ondansetron (Zofran), quiNIDine, thio- No dose adjustment. Decreased effect,
pental (Pentothal), vinBLAStine (Vel- increased sensitivity to hypokalemia/vol-
ban), vinCRIStine (Oncovin), vinorelbine ume depletion in cirrhosis.
(Navelbine).
SIDE EFFECTS
IV COMPATIBILITIES Expected: Increased urinary frequency/
Amiodarone (Cordarone), bumetanide volume. Frequent: Nausea, dyspepsia,
(Bumex), calcium gluconate, cimetidine abdominal cramps, diarrhea or consti-
(Tagamet), dexmedetomidine (Precedex), pation, electrolyte disturbances. Occa- F
heparin, HYDROmorphone (Dilaudid), sional: Dizziness, light-headedness,
lidocaine, lipids, morphine, nitroglycerin, head­ache, blurred vision, paresthesia,
norepinephrine (Levophed), potassium photosensitivity, rash, fatigue, blad-
chloride, propofol (Diprivan). der spasm, restlessness, diaphoresis.
Rare: Flank pain.
INDICATIONS/ROUTES/DOSAGE
Edema, HF ADVERSE EFFECTS/TOXIC
PO: ADULTS, ELDERLY: Initially, 20–80 REACTIONS
mg/dose; may increase by 20–40 mg/ Vigorous diuresis may lead to profound
dose q6–8h. May titrate up to 600 mg/ water loss/electrolyte depletion, resulting
day in severe edematous states. CHIL- in hypokalemia, hyponatremia, dehydra-
DREN: Initially, 2 mg/kg/dose. May tion. Sudden volume depletion may result
increase by 1–2 mg/kg/dose at 6–8 hr in increased risk of thrombosis, circulatory
intervals. Maximum: 6 mg/kg/dose. collapse, sudden death. Acute hypotensive
NEONATES: 1 mg/kg/dose 1–2 times/day. episodes may occur, sometimes several
IV, IM: ADULTS, ELDERLY: 20–40 mg/ days after beginning therapy. Ototoxicity
dose; may increase by 20 mg/dose q1–2h. (deafness, vertigo, tinnitus) may occur,
Maximum single dose: 160–200 mg. esp. in pts with severe renal impairment.
CHILDREN: Initially, 1 mg/kg/dose. May Can exacerbate diabetes mellitus, systemic
increase by 1 mg/kg/dose no sooner than lupus erythematosus, gout, pancreatitis.
2 hrs after previous dose. Maximum: 6 Blood dyscrasias have been reported.
mg/kg/dose. NEONATES: 1–2 mg/kg/
dose q12–24h. NURSING CONSIDERATIONS
IV infusion: ADULTS, ELDERLY: Load- BASELINE ASSESSMENT
ing dose bolus of 40–100 mg over 1–2 Check vital signs, esp. B/P, pulse, for hy-
min, followed by infusion of 10–40 mg/ potension before administration. Assess
hr; repeat loading dose before increas- baseline renal function, serum electro-
ing infusion rate. Maximum: 80–160 lytes, esp. serum sodium, potassium.
mg/hr. CHILDREN: 0.05 mg/kg/hr; titrate Assess skin turgor, mucous membranes
to desired effect. NEONATES: Initially, for hydration status; observe for edema.
0.2 mg/kg/hr. May increase by 0.1 mg/ Assess muscle strength, mental status.
kg/hr q12–24h. Maximum: 0.4 mg/ Note skin temperature, moisture. Obtain
kg/hr. baseline weight. Initiate I&O monitor-
Hypertension ing. Auscultate lung sounds. In pts with
PO: ADULTS, ELDERLY: 20–40 mg twice hepatic cirrhosis and ascites, consider
daily. Range: 20–80 mg/day in 2 divided giving initial doses in a hospital setting.
doses. INTERVENTION/EVALUATION
Dosage in Renal Impairment Monitor B/P, vital signs, serum electro-
Avoid use in oliguric states. lytes, I&O, weight. Note extent of diuresis.

Canadian trade name Non-Crushable Drug High Alert drug


518 furosemide
Watch for symptoms of electrolyte imbal- PATIENT/FAMILY TEACHING
ance: Hypokalemia may result in changes • Expect increased frequency, volume of
in muscle strength, tremor, muscle urination. • Report palpitations, signs of
cramps, altered mental status, cardiac electrolyte imbalances (noted previously),
arrhythmias; hyponatremia may result in hearing abnormalities (sense of fullness in
confusion, thirst, cold/clammy skin. Con- ears, tinnitus). • Eat foods high in potas-
sider potassium supplementation if hypo- sium such as whole grains (cereals), le-
kalemia occurs. gumes, meat, bananas, apricots, orange
juice, potatoes (white, sweet), rai-
F sins. • Avoid sunlight, sunlamps.

underlined – top prescribed drug


gabapentin 519
LIFESPAN CONSIDERATIONS
gabapentin Pregnancy/Lactation: Crosses placenta,
excreted in breast milk. Children: Safety
ga-ba-pen-tin and efficacy not established in pts 3 yrs and
(Gralise, Horizant, Neurontin) younger. Elderly: Age-related renal im-
Do not confuse Neurontin with pairment may require dosage adjustment.
Motrin, Neoral, nitrofurantoin,
Noroxin, or Zarontin. INTERACTIONS
uCLASSIFICATION DRUG: CNS depressants (e.g., alcohol,
morphine, tapentadol, zolpidem) may
PHARMACOTHERAPEUTIC: Gamma- increase CNS depression. HERBAL: Herb-
aminobutyric acid analogue. CLINI- als with sedative properties (e.g., G
CAL: Anticonvulsant, antineuralgic.
chamomile, kava kava, valerian) may
increase CNS depression. FOOD: None
USES known. LAB VALUES: May alter serum
glucose; WBC count. May increase serum
Neurontin: Adjunct in treatment of par-
alkaline phosphatase, ALT, AST, bilirubin.
tial seizures (with or without secondary
generalized seizures) in children 3 yrs AVAILABILITY (Rx)
and older and adults. Management of
Capsules: 100 mg, 300 mg, 400 mg. Oral
postherpetic neuralgia (PHN). Hori-
Solution: 250 mg/5 mL. Tablets: 600
zant: Treatment of moderate to severe
mg, 800 mg. Tablets: (Gralise): 300 mg,
primary restless legs syndrome (RLS),
600 mg.
PHN. Gralise: Management of PHN. OFF-
LABEL: Treatment of neuropathic pain, Tablets: (Extended-Release [Hori-
diabetic peripheral neuropathy, vasomo- zant]): 300 mg, 600 mg.
tor symptoms, fibromyalgia, postopera-
tive pain adjunct. ADMINISTRATION/HANDLING
PO
PRECAUTIONS Immediate-release/solution • Give
Contraindications: Hypersensitivity to ga- without regard to meals; may give with
bapentin. Cautions: Severe renal impair- food to avoid, reduce GI upset. • Swal-
ment, elderly, history of suicidal behav- low extended-release tablets whole; do not
ior; substance abuse. break, crush, dissolve, or divide. Take with
evening meal.
ACTION
Binds to gabapentin binding sites in brain INDICATIONS/ROUTES/DOSAGE
and may modulate release of excitatory Note: When given 3 times/day, maxi-
neurotransmitters, which participates in mum time between doses should not ex-
epileptogenesis and nociception. Thera- ceed 12 hrs. If treatment is discontinued
peutic Effect: Reduces seizure activity, or anticonvulsant therapy is added, do so
neuropathic pain. gradually over at least 1 wk (reduces risk
of loss of seizure control).
PHARMACOKINETICS
Adjunctive Therapy for Seizure Control
Well absorbed from GI tract (not affected
PO: ADULTS, ELDERLY, CHILDREN 13 YRS
by food). Protein binding: less than 5%.
AND OLDER: Initially, 300 mg 3 times/day.
Widely distributed. Crosses blood-brain
May titrate dosage. Range: 900–1,800 mg/
barrier. Primarily excreted unchanged in
day in 3 divided doses. Maximum: 3,600
urine. Removed by hemodialysis. Half-
mg/day. CHILDREN 3–12 YRS: Initially,
life: 5–7 hrs (increased in renal im-
10–15 mg/kg/day in 3 divided doses. May
pairment, elderly).
titrate up to 25–35 mg/kg/day (for
Canadian trade name Non-Crushable Drug High Alert drug
520 gabapentin
children 5–12 yrs) and 40 mg/kg/day (for SIDE EFFECTS
children 3–4 yrs). Maximum: 50 mg/ Frequent (19%–10%): Fatigue, drowsiness,
kg/day. dizziness, ataxia. Occasional (8%–3%):
Nystagmus, tremor, diplopia, rhinitis,
Adjunctive Therapy for Neuropathic Pain
weight gain, peripheral edema. Rare (less
PO: ADULTS, ELDERLY: (Immediate-
than 2%): Anxiety, dysarthria, memory
Release): Initially, 100–300 mg 1–3
loss, dyspepsia, pharyngitis, myalgia.
times/day. May increase up to 1,200
mg 3 times/day. (Extended-Release): ADVERSE EFFECTS/TOXIC
Initially, 300 mg at bedtime. May in- REACTIONS
crease up to target dose of 900–3,600
Abrupt withdrawal may increase seizure
G mg once daily.
frequency, increase risk of suicidal be-
Postherpetic Neuralgia havior/thoughts. Overdosage may result
PO: ADULTS, ELDERLY: (Neurontin): in slurred speech, drowsiness, lethargy,
300 mg once on day 1, 300 mg twice diarrhea. Drug reaction with eosino-
daily on day 2, and 300 mg 3 times/day philia and systemic symptoms (multi-
on day 3 as needed. Range: 1,800–3,600 organ hypersensitivity) was reported.
mg/day. (Gralise): 300 mg once on Hypersensitivity reaction, including ana-
day 1; 600 mg once on day 2; 900 mg phylaxis and angioedema, can occur at
once daily on days 3–6; 1,200 mg once any time.
daily on days 7–10; 1,500 mg once daily
on days 11–14; then 1,800 mg once
NURSING CONSIDERATIONS
daily. (Horizant): 600 mg once daily in BASELINE ASSESSMENT
AM for 3 days, then increase to 600 mg Review history of seizure disorder (type,
twice daily. onset, intensity, frequency, duration,
LOC). Assess location, intensity of neural-
RLS
gia/neuropathic pain. Question history of
PO: ADULTS, ELDERLY: (Horizant): 600
renal impairment.
mg once daily at about 5 PM.
INTERVENTION/EVALUATION
Dosage in Renal Impairment
Provide safety measures as needed. Mon-
Dosage and frequency are modified
itor seizure frequency/duration, renal
based on creatinine clearance.
function, weight, behavior in children.
Dosage in Hepatic Impairment Monitor for signs/symptoms of depres-
No dose adjustment. sion, suicidal tendencies, other unusual
behavior; hypersensitivity reaction.

Creatinine Neurontin Dosage Gralise Dosage Horizant Dosage


Clearance (Immediate- (Extended-release)
release) RLS PHN
30–59 mL/min 200–700 mg q12h 600–1,800 mg 300–600 mg/day Same
once/day
16–29 mL/min 200–700 mg Not recommended 300 mg/day Same
once daily
Less than 16 100–300 mg Not recommended 300 mg q48h Same
mL/min once daily
Hemodialysis 125–350 mg Not recommended Not 300–600 mg
following HD recommended ­following
HD

underlined – top prescribed drug


galantamine 521
PATIENT/FAMILY TEACHING ACTION
• Use only as prescribed; do not Elevates acetylcholine concentrations in
abruptly stop taking drug (may increase cerebral cortex by slowing degeneration of
seizure frequency). • Avoid tasks that acetylcholine released by still intact cholin-
require alertness, motor skills until re- ergic neurons. May increase serotonin/glu-
sponse to drug is established. • Avoid tamate levels. Therapeutic Effect: Slows
alcohol. • Carry identification card/ progression of Alzheimer’s disease.
bracelet to note seizure disorder/anti-
convulsant therapy. • Report suicidal PHARMACOKINETICS
ideation, depression, unusual behavioral Rapidly, completely absorbed from GI
changes (esp. with changes in dosage), tract. Protein binding: 18%. Distributed
worsening of seizure activity or loss of to blood cells; binds to plasma proteins, G
seizure control. Seek medical attention mainly albumin. Metabolized in liver. Ex-
for allergic reactions including difficulty creted in urine. Half-life: 7 hrs.
breathing, coughing, wheezing, throat
tightness, swelling of face or tongue. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if drug
crosses placenta or is distributed in breast
galantamine milk. Children: Not prescribed for this
pt population. Elderly: No age-related
gal-an-ta-meen precautions noted, but use is not recom-
(Razadyne, Razadyne ER, Reminyl mended in those with severe hepatic/renal
ER ) impairment (creatinine clearance less than
Do not confuse Razadyne with 9 mL/min).
Rozerem, or Reminyl with
Amaryl. INTERACTIONS
DRUG: Anticholinergic agents may
uCLASSIFICATION decrease levels/effects. HERBAL: None
PHARMACOTHERAPEUTIC: Acetyl- significant. FOOD: None known. LAB VAL-
cholinesterase inhibitor (central). UES: None significant.
CLINICAL: Antidementia.
AVAILABILITY (Rx)
Oral Solution: 4 mg/mL. T­ablets: (Raza-
USES dyne): 4 mg, 8 mg, 12 mg.
Treatment of mild to moderate dementia Capsules: (Extended-Release [Razadyne
of Alzheimer’s type. OFF-LABEL: Diabetic ER]): 8 mg, 16 mg, 24 mg.
neuropathy, neuropathic pain, postop-
erative pain (adjunct), hot flashes. ADMINISTRATION/HANDLING
PO
PRECAUTIONS • Give tablet or solution with morning
Contraindications: Hypersensitivity to and evening meals. • Mix oral solution
galantamine. Cautions: Moderate renal/ with nonalcoholic beverage, take immedi-
hepatic impairment (not recommended ately. • Extended-release capsule should
in severe impairment), history of ulcer be given with breakfast. Swallow whole.
disease, asthma, COPD, bladder outflow Do not break, crush, cut, or divide.
obstruction, supraventricular cardiac
conduction conditions (except with pace- INDICATIONS/ROUTES/DOSAGE
maker), seizure disorder, concurrent Note: If therapy interrupted for 3 or
medications that slow cardiac conduction more days, restart at lowest dose; then
through SA or AV node. Elderly with low increase gradually.
body weight and/or serious co-morbidities.
Canadian trade name Non-Crushable Drug High Alert drug
522 ganciclovir
Alzheimer’s Disease disturbances (nausea, vomiting, diar-
PO: (Immediate-Release Tablets, rhea, anorexia, weight loss).
Oral Solution): ADULTS, ELDERLY: Ini-
tially, 4 mg twice daily (8 mg/day). After PATIENT/FAMILY TEACHING
a minimum of 4 wks (if well tolerated), • Take with meals (reduces risk of nau-
may increase to 8 mg twice daily (16 mg/ sea). • Avoid tasks that require alert-
day). After another 4 wks, may increase ness, motor skills until response to drug
to 12 mg twice daily (24 mg/day). Range: is established. • Report persistent GI
16–24 mg/day in 2 divided doses. disturbances, excessive salivation, dia-
PO: (Extended-Release): ADULTS, EL- phoresis, excessive tearing, excessive fa-
DERLY: Initially, 8 mg once daily for 4 wks; tigue, insomnia, depression, dizziness,
G then increase to 16 mg once daily for 4 wks increased muscle weakness, palpitations.
or longer. If tolerated, may increase to 24
mg once daily. Range: 16–24 mg once daily.
ganciclovir
Dosage in Renal/Hepatic Impairment
Moderate impairment: Maximum dos- gan-sye-kloe-veer
age is 16 mg/day. Severe impairment: Not (Cytovene)
recommended. j BLACK BOX ALERT jToxicity
presents as neutropenia, thrombo-
SIDE EFFECTS cytopenia, anemia. Studies suggest
Frequent (17%–7%): Nausea, vomiting, di- carcinogenic and teratogenic
effects, inhibition of spermatogen-
arrhea, anorexia, weight loss. Occasional esis. May cause birth defects.
(5%–4%): Abdominal pain, insomnia, Do not confuse Cytovene with
depression, headache, dizziness, fatigue, Cytosar, or ganciclovir with
rhinitis. Rare (less than 3%): Tremors, famciclovir or acyclovir.
constipation, confusion, cough, anxiety,
urinary incontinence. uCLASSIFICATION
PHARMACOTHERAPEUTIC: Synthetic
ADVERSE EFFECTS/TOXIC
REACTIONS nucleoside. CLINICAL: Antiviral.
Overdose may cause cholinergic crisis
(increased salivation, lacrimation, uri- USES
nation, defecation, bradycardia, hypo- Treatment of cytomegalovirus (CMV) ret-
tension, muscle weakness). Treatment initis in immunocompromised pts (e.g.,
aimed at generally supportive measures, HIV), prophylaxis of CMV infection in
use of anticholinergics (e.g., atropine). transplant pts. OFF-LABEL: CMV retinitis.

NURSING CONSIDERATIONS PRECAUTIONS


Contraindications: Hypersensitivity to
BASELINE ASSESSMENT acyclovir, ganciclovir, valganciclovir. Cau-
Assess cognitive, behavioral, functional tions: Neutropenia, thrombocytopenia,
deficits of pt. Obtain baseline serum renal renal impairment, children (long-term
function, LFT. Question history as listed safety not determined due to potential
in Precautions, esp. cardiac conduction for long-term carcinogenic, adverse re-
disorders. productive effects), pregnancy. Absolute
INTERVENTION/EVALUATION
neutrophil count less than 500 cells/mm3,
platelet count less than 25,000 cells/mm3.
Monitor cognitive, behavioral, func-
tional status of pt. Evaluate ECG, periodic ACTION
rhythm strips in pts with underlying ar- Competes with viral DNA polymerase and
rhythmias. Assess for evidence of GI incorporation into growing viral DNA
underlined – top prescribed drug
ganciclovir 523
chains. Therapeutic Effect: Interferes Storage • Store vials at room tempera-
with DNA synthesis, viral replication. ture. Do not refrigerate. • Reconstituted
solution in vial is stable for 12 hrs at
PHARMACOKINETICS room temperature. • After dilution, use
Widely distributed (including CSF and within 24 hrs. • Discard if precipitate
ocular tissue). Protein binding: 1%–2%. forms, discoloration occurs. • Avoid
Excreted primarily in urine. Removed by exposure to skin, eyes, mucous mem-
hemodialysis. Half-life: 1.7–5.8 hrs branes. • Use latex gloves, safety glasses
(increased in renal impairment). during preparation/handling of solu-
tion. • Avoid inhalation. • If solution
LIFESPAN CONSIDERATIONS contacts skin or mucous membranes,
Pregnancy/Lactation: Avoid pregnancy. wash thoroughly with soap and water; G
Female pts of reproductive potential should rinse eyes thoroughly with plain water.
use effective contraception during treat-
ment and for 30 days after discontinuation; IV INCOMPATIBILITIES
male pts should use a barrier contraceptive Aldesleukin (Proleukin), amifostine
during and for at least 90 days after discon- (Ethyol), aztreonam (Azactam), cefepime
tinuation. Do not breastfeed. May resume (Maxipime), cytarabine (ARA-C), DOXOru-
breastfeeding no sooner than 72 hrs after bicin (Adriamycin), fludarabine (Fludara),
the last dose. Children: Safety and efficacy foscarnet (Foscavir), gemcitabine (Gem-
not established in pts younger than 12 yrs. zar), ondansetron (Zofran), piperacillin
Elderly: Age-related renal impairment and tazobactam (Zosyn), sargramostim
may require dosage adjustment. (Leukine), vinorelbine (Navelbine).
INTERACTIONS IV COMPATIBILITIES
DRUG: Bone marrow depressants may Amphotericin B, enalapril (Vasotec),
increase myelosuppression. Imipenem may filgrastim (Neupogen), fluconazole (Di-
increase risk for seizures. HERBAL: None flucan), granisetron (Kytril), propofol
significant. FOOD: None known. LAB VAL- (Diprivan).
UES: May increase serum alkaline phospha-
tase, ALT, AST, bilirubin, BUN, creatinine. INDICATIONS/ROUTES/DOSAGE
AVAILABILITY (Rx) Cytomegalovirus (CMV) Retinitis
Injection, Powder for Reconstitution: (Cy- IV: ADULTS, CHILDREN 3 MOS AND OLDER:
tovene): 500 mg. Solution, Intravenous: 5 mg/kg/dose q12h for 14–21 days, then
500 mg/250 mL. 5 mg/kg/day as a single daily dose or
6 mg/kg 5 days/wk as maintenance therapy.
ADMINISTRATION/HANDLING
Prevention of CMV in Transplant Pts
IV
IV: ADULTS, CHILDREN: 5 mg/kg/dose
Reconstitution • Reconstitute 500-mg q12h for 7–14 days, then 5 mg/kg/day as
vial with 10 mL Sterile Water for Injection a single daily dose or 6 mg/kg 5 days/wk.
to provide concentration of 50 mg/mL; do Duration dependent on clinical condition
not use Bacteriostatic Water (contains and degree of immunosuppression.
parabens, which are incompatible with
ganciclovir). • Further dilute with 100 mL Congenital CMV
D5W, 0.9% NaCl to provide a concentra- IV: NEONATES: 6 mg/kg/dose q12h for 6
tion of 10 mg/mL or less for infusion. wks (if HIV positive, longer duration may
Rate of administration • Administer be considered).
only by IV infusion over at least 1 hr. • Do
not give by IV push or rapid IV infusion Dosage in Renal Impairment
(increases risk of toxicity). Flush line with Dosage and frequency are modified based
0.9% NaCl before and after administration. on creatinine clearance (see table).
Canadian trade name Non-Crushable Drug High Alert drug
524 gefitinib
Dosage
Creatinine Clearance IV Induction IV Maintenance
50–69 mL/min 2.5 mg/kg q12h 2.5 mg/kg q24h
25–49 mL/min 2.5 mg/kg q24h 1.25 mg/kg q24h
10–24 mL/min 1.25 mg/kg q24h 0.625 mg/kg q24h
Less than 10 mL/min 1.25 mg/kg 3 times/wk 0.625 mg/kg 3 times/wk
Hemodialysis (give after HD on HD 1.25 mg/kg q48–72h 0.625 mg/kg q48–72h
days)
Peritoneal dialysis 1.25 mg/kg 3 times/wk 0.625 mg/kg 3 times/wk
Continuous renal replacement therapy
Continuous venovenous hemofiltration 2.5 mg/kg q24h 1.25 mg/kg q24h
Continuous venovenous 2.5 mg/kg q12h 2.5 mg/kg q24h
G hemodialysis/continuous
venovenous hemodiafiltration

Dosage in Hepatic Impairment penia, thrombocytopenia, leukopenia.


No dose adjustment. Obtain periodic ophthalmic examina-
tions. Question pt regarding visual acuity,
SIDE EFFECTS therapeutic improvement, complications.
Frequent (41%–13%): Diarrhea, fever, Assess for rash, pruritus.
nausea, abdominal pain, vomiting. Occa-
sional (11%–6%): Diaphoresis, infection, PATIENT/FAMILY TEACHING
paresthesia, flatulence, pruritus. Rare • Ganciclovir provides suppression, not
(4%–2%): Headache, stomatitis, dyspep- cure, of cytomegalovirus (CMV) retini-
sia, phlebitis. tis. • Frequent blood tests, eye exams
are necessary during therapy due to toxic
ADVERSE EFFECTS/TOXIC nature of drug. • Report any new symp-
REACTIONS tom promptly. • May temporarily or
Hematologic toxicity occurs com- permanently inhibit sperm production in
monly: leukopenia (41%–29% of pts), men, suppress fertility in women. • Bar-
anemia (25%–19% of pts). Intraocular rier contraception should be used during
implant occasionally results in visual and for 90 days after therapy due to mu-
acuity loss, vitreous hemorrhage, reti- tagenic potential.
nal detachment. GI hemorrhage occurs
rarely.
NURSING CONSIDERATIONS gefitinib
BASELINE ASSESSMENT
ge-fi-ti-nib
Obtain baseline CBC, BMP, LFT. Perform (Iressa)
baseline ophthalmic exam. Obtain speci- Do not confuse gefitinib with
mens for support of differential diagnosis erlotinib, dasatinib, imatinib,
(urine, feces, blood, throat) since retinal or lapatinib.
infection is usually due to hematogenous
dissemination. uCLASSIFICATION
INTERVENTION/EVALUATION PHARMACOTHERAPEUTIC: Epider-
Monitor I&O, ensure adequate hydration mal growth factor receptor (EGFR)
(minimum 1,500 mL/24 hrs). Diligently inhibitor. Tyrosine kinase inhibitor.
CLINICAL: Antineoplastic.
evaluate hematology reports for neutro-

underlined – top prescribed drug


gefitinib 525

USES concentration/effect. HERBAL: St. John’s


First-line treatment of metastatic non– wort may decrease effectiveness.
small-cell lung cancer (NSCLC) whose FOOD: Avoid grapefruit products. LAB
tumors have epidermal growth factor re- VALUES: May increase serum AST, ALT,
ceptor (EGFR) exon 19 deletions or exon bilirubin, urine protein.
21 substitution mutations.
AVAILABILITY (Rx)
PRECAUTIONS Tablets: 250 mg.
Contraindications: Hypersensitivity to gefi-
ADMINISTRATION/HANDLING
tinib. Cautions: Hepatic impairment, lung
disease, ocular disease, concurrent admin- • May give without regard to food. •
istration of CYP3A4 inducers and inhibitors. Avoid grapefruit products. • Do not G
crush or cut. Swallow whole or adminis-
ACTION ter as dispersion in water. Gently swirl
Reversibly inhibits epidermal growth fac- glass for up to 20 min and immediately
tor receptor–tyrosine kinase (EGFR-TK), ingest once dispersed.
a key driver in tumor cell growth. EGFR is
INDICATIONS/ROUTES/DOSAGE
expressed on cell surfaces of cancer cells.
Therapeutic Effect: Inhibits tumor cell NSCLC
proliferation and survival. PO: ADULTS, ELDERLY: 250 mg once daily,
with or without food. Continue until dis-
PHARMACOKINETICS ease progression or unacceptable toxicity.
Slowly absorbed following PO adminis- Concomitant Use of CYP3A4 Inducers
tration. Peak plasma levels in 3–7 hrs. Consider increasing dose to 500 mg once
Protein binding: 90%. Metabolized in daily if use of CYP3A4 is unavoidable. If
liver. Excreted primarily in feces (86%). CYP3A4 inducer is discontinued, reduce
Half-life: 48 hrs. dose to 250 mg 7 days after discontinuation.
Dosage in Renal Impairment
LIFESPAN CONSIDERATIONS
No dose adjustment.
Pregnancy/Lactation: Avoid pregnancy.
Use effective contraception during treat- Dosage in Hepatic Impairment
ment and for at least 2 wks after discon- Mild impairment: No dose adjust-
tinuation. Unknown if crosses placenta ment. Moderate to severe impair-
or distributed in breast milk. Must either ment: Use with caution.
discontinue breastfeeding or discontinue
therapy. Children: Safety and efficacy not SIDE EFFECTS
established. Elderly: No age-related pre- Frequent (47%–15%): Skin reactions
cautions noted. (e.g., acne, pruritus, rash, xeroderma),
diarrhea, decreased appetite, vomiting.
INTERACTIONS Occasional (7%–5%): Stomatitis, con-
DRUG: CYP3A4 inhibitors (e.g., clar- junctivitis, blepharitis, dry eye, nail dis-
ithromycin, ketoconazole, ritonavir) orders (e.g., infection).
may increase concentration. CYP3A4
inducers (e.g., carbamazepine, ADVERSE EFFECTS/TOXIC
phenytoin, rifAMPin) may decrease REACTIONS
concentration. H2 antagonists (e.g., Hepatotoxicity, interstitial lung disease,
famotidine), proton pump inhibi- gastrointestinal perforation, severe or
tors (e.g., pantoprazole) may decrease persistent diarrhea, ocular disorders in-
concentration. May increase bleeding risk cluding keratitis, bullous and exfoliative
with warfarin. Antacids may decrease skin disorders.

Canadian trade name Non-Crushable Drug High Alert drug


526 gemcitabine

NURSING CONSIDERATIONS USES


Metastatic breast cancer in combination
BASELINE ASSESSMENT with PACLitaxel. Treatment of locally ad-
Obtain baseline CBC with differential, vanced (stage II, III) or metastatic (stage
serum chemistries, LFT, thyroid function IV) adenocarcinoma of pancreas. In com-
test, PT/INT (if taking warfarin), EGFR bination with CISplatin for treatment of
mutation serostatus. Question possibility locally advanced or metastatic non–small-
of pregnancy or plans of breastfeeding. cell lung cancer (NSCLC). Treatment of
Receive full medication history including advanced ovarian cancer (in combination
vitamins, minerals, herbal products. As- with CARBOplatin) that has relapsed. OFF-
sess visual acuity. LABEL: Treatment of biliary tract carcinoma,
G bladder carcinoma, germ cell tumors (e.g.,
INTERVENTION/EVALUATION
testicular), Hodgkin’s lymphoma, non-
Assess vital signs, oxygen saturation rou- Hodgkin’s lymphoma, cervical cancer.
tinely. Routinely monitor CBC with dif-
ferential, LFT. Worsening cough, fever, PRECAUTIONS
or shortness of breath may indicate in- Contraindications: Hypersensitivity to gem-
terstitial lung disease. Consider ophthal- citabine. Cautions: Renal/hepatic impair-
mologic evaluation for vision changes. ment, pregnancy, elderly, concurrent radia-
Monitor for bruising, hematuria, jaun- tion therapy, impaired pulmonary function.
dice, right upper abdominal pain, weight
loss, or acute infection (fever, diaphore- ACTION
sis, lethargy, productive cough). Monitor Inhibits ribonucleotide reductase, the
for skin lesions. enzyme necessary for catalyzing DNA
PATIENT/FAMILY TEACHING synthesis. Cell-cycle specific for the S-
• Blood levels will be drawn routinely. phase. Therapeutic Effect: Produces
Report urine changes, bloody or clay-col- death of cells undergoing DNA synthesis.
ored stools, upper abdominal pain, nau- PHARMACOKINETICS
sea, vomiting, bruising, fever, cough, dif-
ficulty breathing. • Immediately report Not extensively distributed after IV infu-
any newly prescribed medications, sus- sion (increased with length of infusion).
pected pregnancy, vision changes (eye Protein binding: less than 10%. Me-
pain, bleeding, sensitivity to light), or tabolized intracellularly by nucleoside
persistent diarrhea, dehydration. • Avoid kinases. Excreted primarily in urine.
alcohol. • Avoid grapefruit products. Half-life: Influenced by duration of in-
fusion. Infusion 1 hr or less: 42–94 min;
infusion 3–4 hrs: 4–10.5 hrs.
LIFESPAN CONSIDERATIONS
gemcitabine Pregnancy/Lactation: If possible, avoid
use during pregnancy, esp. first trimester.
jem-sye-ta-been May cause fetal harm. Unknown if distrib-
(Gemzar ) uted in breast milk. Breastfeeding not rec-
Do not confuse gemcitabine ommended. Children: Safety and efficacy
with gemtuzumab, Gemzar with not established. Elderly: Increased risk of
Zinecard. hematologic toxicity.

uCLASSIFICATION
INTERACTIONS
DRUG: Bone marrow depressants
PHARMACOTHERAPEUTIC: Antime-
(e.g., cladribine) may increase risk of
tabolite. CLINICAL: Antineoplastic.
myelosuppression. Live virus vaccines
underlined – top prescribed drug
gemcitabine 527
may potentiate virus replication, increase INDICATIONS/ROUTES/DOSAGE
vaccine side effects, decrease pt’s anti- b ALERT c Dosage is individualized based
body response to vaccine. HERBAL: Echi- on clinical response, tolerance to adverse
nacea may decrease effects. FOOD: None effects. When used in combination therapy,
known. LAB VALUES: May increase se- consult specific protocols for optimum dos-
rum BUN, alkaline phosphatase, bilirubin, age, sequence of drug administration.
creatinine, ALT, AST. May decrease Hgb,
Hct, leukocyte count, platelet count. Breast Cancer (Metastatic)
IV: ADULTS, ELDERLY: (in combination
AVAILABILITY (Rx) with PACLitaxel): 1,250 mg/m2 over 30
Injection, Powder for Reconstitution: min on days 1 and 8 of each 21-day cycle.
200-mg, 1-g, 2-g vials. Injection, Solution: G
38 mg/mL, 100 mg/mL. Non–Small-Cell Lung Cancer (NSCLC)
(Inoperable, Locally Advanced, or
ADMINISTRATION/HANDLING Metastatic)
IV: ADULTS, ELDERLY, CHILDREN: (in com-
IV
bination with CISplatin): 1,000 mg/m2 on
Reconstitution • Use gloves when days 1, 8, and 15, repeated every 28 days;
handling/preparing. • Reconstitute or 1,250 mg/m2 on days 1 and 8. Repeat
with 0.9% NaCl injection without preser- every 21 days.
vative to provide concentration of 38 mg/
mL. • Shake to dissolve. Further di- Ovarian Cancer (Advanced)
luted with 50–500 mL 0.9% NaCl to a IV: ADULTS, ELDERLY: (in combination
concentration as low as 0.1 mg/mL. with CARBOplatin): 1,000 mg/m2 on days
Rate of administration • Infuse over 1 and 8 of each 21-day cycle.
30 min. • Infusion time greater than 60 Pancreatic Cancer (Locally Advanced or
min increases toxicity. Metastatic)
Storage • Store at room temperature IV: ADULTS: 1,000 mg/m2 once wkly for
(refrigeration may cause crystalliza- up to 7 wks or until toxicity necessitates
tion). • Reconstituted vials or diluted decreasing dosage or withholding the
solutions are stable for 24 hrs at room dose, followed by 1 wk of rest. Subsequent
temperature. Do not refrigerate. cycles should consist of once-wkly dose
for 3 consecutive wks out of every 4 wks.
IV INCOMPATIBILITIES
Acyclovir (Zovirax), amphotericin B Dosage in Renal/Hepatic Impairment
(Fungizone), cefotaxime (Claforan), fu- No dose adjustment.
rosemide (Lasix), ganciclovir (Cytovene),
imipenem/cilastatin (Primaxin), irinote- Dosage Reduction
can (Camptosar), methotrexate, methyl- Pancreatic Cancer, Non–Small-Cell Lung
PREDNISolone (SOLU-Medrol), mitoMY- Cancer (NSCLC)
cin (Mutamycin), piperacillin/tazobactam Dosage adjustments should be based on
(Zosyn), prochlorperazine (Compazine). granulocyte count and platelet count, as
follows:
IV COMPATIBILITIES
Bumetanide (Bumex), calcium gluconate, Absolute Platelet
dexamethasone (Decadron), diphenhy- Granulocyte Count % of Full
drAMINE (Benadryl), DOBUTamine (Do- Counts (cells/mm3) (cells/mm3) Dose
butrex), DOPamine (Intropin), granis- 1,000 100,000 100
etron (Kytril), heparin, hydrocortisone 500–999 50,000–99,000 75
(Solu-CORTEF), LORazepam (Ativan), on- Less than Less than Hold
500 or 50,000
dansetron (Zofran), potassium chloride.

Canadian trade name Non-Crushable Drug High Alert drug


528 gemfibrozil
Breast Cancer of pulmonary disease, hepatic/renal im-
Absolute pairment. Offer emotional support.
Granulocyte
INTERVENTION/EVALUATION
Counts (cells/ Platelet Count % of Full
mm3) (cells/mm3) Dose Assess all lab results prior to each dose.
Equal to or Greater than 100 Monitor for dyspnea, fever, pruritic rash,
greater than 75,000 dehydration. Assess oral mucosa for ery-
1,200 and thema, ulceration at inner margin of lips,
1,000–1,199 or 50,000–75,000 75 sore throat, difficulty swallowing (stoma-
700–999 and Equal to or 50 titis). Assess skin for rash. Monitor daily
greater than pattern of bowel activity, stool consis-
50,000 tency. Provide antiemetics as needed.
G Less than 700 or Less than Hold
50,000 PATIENT/FAMILY TEACHING
• Avoid crowds, exposure to infection. •
Ovarian Cancer Maintain strict oral hygiene. • Promptly
Absolute report fever, sore throat, signs of local infec-
Granulocyte tion, easy bruising, rash, yellowing of skin
Counts (cells/ Platelet Count % of Full or eyes. • Report nausea or vomiting that
mm3) (cells/mm3) Dose continues at home.
1,500 or 100,000 or 100
greater and greater
1,000–1,499
and/or
75,000–99,999 50
gemfibrozil
Less than 1,000 Less than Hold
and/or 75,000 jem-fye-broe-zil
(Lopid)
Do not confuse Lopid with Lev-
SIDE EFFECTS bid, Lipitor, Lodine, or Slo-Bid.
Frequent (69%–20%): Nausea, vomiting,
generalized pain, fever, mild to moderate uCLASSIFICATION
pruritic rash, mild to moderate dyspnea, PHARMACOTHERAPEUTIC: Fibric
constipation, peripheral edema. Occa- acid derivative. CLINICAL: Antihy-
sional (19%–10%): Diarrhea, petechiae, perlipidemic.
alopecia, stomatitis, infection, drowsiness,
paresthesia. Rare: Diaphoresis, rhinitis,
insomnia, malaise. USES
Treatment of hypertriglyceridemia in
ADVERSE EFFECTS/TOXIC Fredrickson types IV and V hyperlipid-
REACTIONS emia in pts who are at greater risk for
Severe myelosuppression (anemia, thro­ pancreatitis and those who have not re-
mbocytopenia, leukopenia) occurs com- sponded to dietary intervention. Reduce
monly. risk of coronary heart disease (CHD)
development in Fredrickson type IIb pts
NURSING CONSIDERATIONS without symptoms who have decreased
BASELINE ASSESSMENT HDL, increased LDL, increased triglyc-
Obtain baseline CBC, renal function, LFT, erides.
and periodically thereafter (CBC, plate- PRECAUTIONS
lets before each dose). Drug should be
suspended or dosage modified if myelo- Contraindications: Hypersensitivity to
suppression is detected. Question history gemfibrozil. Hepatic impairment (includ-
ing primary biliary cirrhosis), preexisting
underlined – top prescribed drug
gemfibrozil 529
gallbladder disease, severe renal impair- ADMINISTRATION/HANDLING
ment, concurrent use with dasabuvir, re- PO
paglinide or simvastatin. Cautions: Con- • Give 30 min before morning and eve-
current use with statins, mild to moderate ning meals.
renal impairment. anticoagulant therapy
(e.g., warfarin). INDICATIONS/ROUTES/
DOSAGE
ACTION
Hyperlipidemia/Hypertriglyceridemia
Exact mechanism of action unknown. PO: ADULTS, ELDERLY: 600 mg twice
Can inhibit lipolysis of fat in adipose daily 30 min before breakfast and dinner.
tissue, decrease hepatic uptake of free
fatty acids (reduces hepatic triglyceride Dosage in Renal Impairment G
production), or inhibit hepatic secretion Use caution. Contraindicated in severe
of very low-density lipoprotein (VLDL). impairment.
Therapeutic Effect: Lowers serum
cholesterol, triglycerides (decreases Dosage in Hepatic Impairment
VLDL, LDL; increases HDL). Contraindicated.

PHARMACOKINETICS SIDE EFFECTS


Well absorbed from GI tract. Protein Frequent (20%): Dyspepsia. Occasional
binding: 99%. Metabolized in liver. Pri- (10%–2%): Abdominal pain, diarrhea,
marily excreted in urine. Not removed by nausea, vomiting, fatigue. Rare (less than
hemodialysis. Half-life: 1.5 hrs. 2%): Constipation, acute appendicitis,
vertigo, headache, rash, pruritus, altered
LIFESPAN CONSIDERATIONS taste.
Pregnancy/Lactation: Unknown if drug
crosses placenta or is distributed in breast ADVERSE EFFECTS/TOXIC
milk. Decision to discontinue breastfeed- REACTIONS
ing or drug should be based on potential Cholelithiasis, cholecystitis, acute appen-
for serious adverse effects. Children: Not dicitis, pancreatitis, malignancy occur
recommended in pts younger than 2 yrs rarely.
(cholesterol necessary for normal develop-
ment). Elderly: Age-related renal impair- NURSING CONSIDERATIONS
ment may require dosage adjustment. BASELINE ASSESSMENT

INTERACTIONS Obtain diet history, esp. fat/alcohol


consumption. Obtain serum glucose,
DRUG: Statins (e.g., atorvastatin, triglyceride, cholesterol, LFT. Question
simvastatin) may increase risk for my- history of hepatic/renal impairment,
opathy/rhabdomyolysis. May increase cholecystectomy. Receive full medica-
effects of repaglinide, warfarin. Bile tion history and screen for contraindi-
acid–binding resins (e.g., colesti- cations.
pol) may decrease concentration. May
increase adverse effects of ezetimibe. INTERVENTION/EVALUATION
HERBAL: None significant. FOOD: None Monitor LDL, VLDL, serum triglycerides,
known. LAB VALUES: May increase serum cholesterol lab results for therapeutic
alkaline phosphatase, bilirubin, creatine response. Monitor daily pattern of bowel
kinase, LDH, ALT, AST. May decrease Hgb, activity, stool consistency. Assess for rash,
Hct, leukocyte counts, serum potassium. pruritus. Question for headache, dizzi-
ness. Monitor LFT, hematology tests. As-
AVAILABILITY (Rx) sess for abdominal pain, esp. right upper
Tablets: 600 mg. quadrant or epigastric pain suggestive of
Canadian trade name Non-Crushable Drug High Alert drug
530 gentamicin
adverse gallbladder effects. Monitor se- Elderly, neonates due to renal insufficiency
rum glucose in pts receiving insulin, oral or immaturity, neuromuscular disorders
antihyperglycemics. (potential for respiratory depression),
vestibular or cochlear impairment, renal
PATIENT/FAMILY TEACHING
impairment, hypocalcemia, myasthenia
• Follow special diet (important part of gravis. Pediatric pts on extracorporeal
treatment). • Take before meals. • Pe- membrane oxygenation.
riodic lab tests are essential part of ther-
apy. • Report pronounced dizziness, ACTION
blurred vision, abdominal pain, diarrhea, Interferes with bacterial protein syn-
nausea, vomiting. thesis. Binds to 30S ribosomal subunit,
G causing a defective cell membrane.
Therapeutic Effect: Bactericidal.
gentamicin PHARMACOKINETICS
Rapid, complete absorption after IM
jen-ta-mye-sin administration. Protein binding: less
j BLACK BOX ALERT jAmino- than 30%. Widely distributed (does not
glycoside antibiotics may cause cross blood-brain barrier, low concen-
neurotoxicity, nephrotoxicity. Risk
of ototoxicity directly proportional trations in CSF). Excreted unchanged in
to dosage, duration of treatment; urine. Removed by hemodialysis. Half-
ototoxicity usually is irreversible, life: 2–4 hrs (increased in renal im-
precipitated by tinnitus, vertigo. pairment, neonates; decreased in cystic
May cause fetal harm if given dur- fibrosis, burn, or febrile pts).
ing pregnancy.
Do not confuse gentamicin with LIFESPAN CONSIDERATIONS
vancomycin. Pregnancy/Lactation: Readily crosses
uCLASSIFICATION placenta; unknown if distributed in
breast milk. Children: Caution in neo-
PHARMACOTHERAPEUTIC: Amino-
nates: Immature renal function increases
glycoside. CLINICAL: Antibiotic. half-life and toxicity. Elderly: Age-re-
lated renal impairment may require dos-
age adjustment.
USES
Parenteral: Treatment of infections INTERACTIONS
susceptible to Pseudomonas, Proteus, DRUG: Nephrotoxic (e.g., furose-
Serratia, and other gram-negative or- mide, IV contrast dye), ototoxic
ganisms and gram-positive Staphylococ- medications (e.g., CISplatin, cyclo-
cus including skin/skin structure, bone, SPORINE, foscarnet, furosemide,
joint, respiratory tract, intra-abdominal, mannitol) may increase risk of neph-
complicated urinary tract, acute pelvic rotoxicity, ototoxicity. HERBAL: None
infections; burns; septicemia; meningi- significant. FOOD: None known. LAB
tis. Ophthalmic: Ophthalmic infections VALUES: May increase serum BUN, cre-
caused by susceptible bacteria. OFF-LA- atinine, bilirubin, LDH, ALT, AST. May de-
BEL: Surgical (preoperative) prophylaxis. crease serum calcium, magnesium, po-
tassium, sodium. Therapeutic serum
PRECAUTIONS level: peak: 4–10 mcg/mL; trough: 0.5–
Contraindications: Hypersensitivity to gen­ 2 mcg/mL. Toxic serum level: peak:
tamicin, other aminoglycosides (cross- greater than 10 mcg/mL; trough: greater
sensitivity) or their components. Cautions: than 2 mcg/mL.

underlined – top prescribed drug


gentamicin 531

AVAILABILITY (Rx) (Hespan), IDArubicin (Idamycin), indo-


Injection, Infusion: 60 mg/50 mL, 80 methacin (Indocin), propofol (Diprivan).
mg/50 mL, 80 mg/100 mL, 100 mg/50
IV COMPATIBILITIES
mL, 100 mg/100 mL, 120 mg/100 mL. In-
jection, Solution: 10 mg/mL, 40 mg/mL. Amiodarone (Cordarone), dexmedeto-
Ointment, Ophthalmic: 0.3%. Solution, midine (Precedex), dilTIAZem (Cardi-
Ophthalmic: (Gentak): 0.3%. zem), enalapril (Vasotec), filgrastim
(Neupogen), HYDROmorphone (Di-
ADMINISTRATION/HANDLING laudid), insulin, LORazepam (Ativan),
magnesium sulfate, midazolam (Versed),
IV morphine, multivitamins.
Reconstitution • Dilute with 50–100 G
mL D5W or 0.9% NaCl. Amount of diluent INDICATIONS/ROUTES/DOSAGE
for infants, children depends on individ- b ALERT c Space parenteral doses
ual needs. evenly around the clock. Dosage based
Rate of administration • Infuse over on ideal body weight. Peak, trough levels
30–60 min for adults, older children; are determined periodically to maintain
over 60–120 min for infants, young chil- desired serum concentrations and mini-
dren. mize risk of toxicity.
Storage • Store vials at room temper-
Usual Parenteral Dosage
ature. • Solution appears clear or
IM, IV: ADULTS, ELDERLY: (Conventional):
slightly yellow. • Intermittent IV infu-
sion (piggyback) is stable for 48 hrs at 3–5 mg/kg/day in divided doses q8h.
(Once Daily): 5–7 mg/kg/dose q24h. CHIL-
room temperature or refrigerated.
DREN 5 YRS AND OLDER: 2–2.5 mg/kg/
• Discard if precipitate forms.
dose q8h. INFANTS, CHILDREN YOUNGER
IM THAN 5 YRS: 2.5 mg/kg/dose q8h.
• To minimize discomfort, give deep IM NEONATES (MORE THAN 2 KG): PNA 8–28
slowly. • Less painful if injected into glu- days: 4–5 mg/kg/dose q24h; PNA 7 days
teus maximus than lateral aspect of thigh. or less: 4 mg/kg/dose q24h. (1–2 KG): PNA
8–28 days: 5 mg/kg/dose q36h; PNA 7 days
Ophthalmic or less: 5 mg/kg/dose q48h. (LESS THAN 1
• Place gloved finger on lower eyelid KG): PNA 15–28 days: 5 mg/kg/dose q36h;
and pull out until a pocket is formed be- PNA 14 days or less: 5 mg/kg/dose q48h.
tween eye and lower lid. • Place pre-
scribed number of drops or 14–12 inch Hemodialysis (HD)
ointment into pocket. Instruct pt to close Note: Administer after HD on dialysis
eye gently for 1–2 min (so that medica- days.
tion will not be squeezed out of the Loading dose: 2–3 mg/kg, then 1 mg/
sac). • Solution: Instruct pt to apply kg q48–72h for mild UTI or synergy
digital pressure to lacrimal sac at inner (consider redose for pre- or post-HD
canthus for 1 min to minimize systemic concentrations less than 1 mg/L); 1–1.5
absorption. • Ointment: Instruct pt to mg/kg q48–72h for moderate to severe
roll eyeball to increase contact area of UTI (consider redose for pre-HD con-
drug to eye. • Remove excess solution centration less than 1.5–2 mg/L or post-
or ointment around eye with tissue. HD concentrations less than 1 mg/L);
1.5–2 mg/kg q48–72h for systemic
IV INCOMPATIBILITIES gram-negative rod infection (consider
Allopurinol (Aloprim), amphotericin B redose for pre-HD concentration less
complex (Abelcet, AmBisome, Amphotec), than 3–5 mg/L or post-HD concentra-
furosemide (Lasix), heparin, heta-starch tions less than 2 mg/L).

Canadian trade name Non-Crushable Drug High Alert drug


532 gentamicin
Continuous Renal Replacement Therapy Burning, tearing, itching, blurred vision.
(CRRT) Rare: Alopecia, hypertension, fatigue.
Loading dose: 2–3 mg/kg, then 1 mg/
kg q24–36h for mild UTI or synergy ADVERSE EFFECTS/TOXIC
(redose when concentration less than REACTIONS
1 mg/L); 1–1.5 mg/kg q24–36h for Nephrotoxicity (increased serum BUN,
moderate to severe UTI (redose when creatinine; decreased creatinine clear-
concentration less than 1.5–2 mg/L); ance) may be reversible if drug is stopped
1.5–2.5 mg/kg q24–48h for systemic at first sign of symptoms. Irreversible
gram-negative infection (redose when ototoxicity (tinnitus, dizziness, dimin-
concentration less than 3–5 mg/L). ished hearing), neurotoxicity (headache,
G dizziness, lethargy, tremor, visual dis-
Usual Ophthalmic Dosage turbances) occur occasionally. Risk in-
Ophthalmic ointment: ADULTS, EL- creases with higher dosages, prolonged
DERLY: Apply 12-inch strip to conjuncti- therapy, or if solution is applied directly
val sac 2–3 times/day. to mucosa. Superinfections, particularly
Ophthalmic solution: ADULTS, EL- with fungi, may result from bacterial im-
DERLY, CHILDREN: 1–2 drops q2–4h up balance via any route of administration.
to 2 drops/hr. Ophthalmic application may cause pares-
Dosage in Renal Impairment
thesia of conjunctiva, mydriasis.
Adults NURSING CONSIDERATIONS
Creatinine Conventional Once-Daily
Clearance Dosage Dosage BASELINE ASSESSMENT
Greater q8h q24h Dehydration must be treated before begin-
than 60 ning parenteral therapy. Establish baseline
mL/mil hearing acuity. Question for history of aller-
41–60 mL/ q12h q36h gies, esp. aminoglycosides, sulfites (para-
min bens for topical/ophthalmic routes). Screen
20–40 mL/ q24h q48h
min
for risk of acute kidney injury, esp. pts at risk
Less than Loading dose, Monitor for renal failure (baseline renal insufficiency,
20 mL/ then monitor levels elderly, HF, hypertension, septic shock).
min levels to de-
INTERVENTION/EVALUATION
termine dos-
age interval Monitor I&O (maintain hydration), uri-
nalysis, BUN, creatinine. Be alert to oto-
Children toxic, neurotoxic symptoms (see Adverse
Conventional Effects/Toxic Reactions). Check IM injec-
Creatinine Clearance Dosage tion site for induration. Evaluate IV site
Greater than 50 mL/min q8h for phlebitis (heat, pain, red streaking
30–50 mL/min q12–18h over vein). Assess for rash (Ophthal-
10–29 mL/min q18–24h mic: redness, burning, itching, tearing).
Less than 10 mL/min q48–72h
Be alert for superinfection (genital/anal
pruritus, changes in oral mucosa, diar-
Dosage in Hepatic Impairment rhea). When treating pts with neuro-
Monitor plasma concentrations. muscular disorders, assess respiratory
response carefully. Therapeutic serum
SIDE EFFECTS level: peak: 4–10 mcg/mL; peak levels
Occasional: IM: Pain, induration at in- are 2–3 times greater with once-daily
jection site. IV: Phlebitis, thrombophle- dosing; trough: 0.5–2 mcg/mL. Toxic
bitis, hypersensitivity reactions (fever, serum level: peak: greater than 10 mcg/
pruritus, rash, urticaria). Ophthalmic: mL; trough: greater than 2 mcg/mL.
underlined – top prescribed drug
gilteritinib 533
PATIENT/FAMILY TEACHING prolongation (congenital long QT syn-
• Discomfort may occur with IM injec- drome, HF, QT interval–prolonging med-
tion. • Blurred vision, tearing may oc- ications, hypokalemia, hypomagnese-
cur briefly after each ophthalmic mia); concomitant use of P-gp inhibitors,
dose. • Report any hearing, visual, bal- strong CYP3A inhibitors, strong CYP3A
ance, urinary problems, even after ther- inducers; history of GI perforation, pan-
apy is completed. • Ophthalmic: Re- creatitis.
port if tearing, redness, irritation
continues. ACTION
Inhibits multiple tyrosine kinases includ-
ing FLT3 receptor signaling and cellular
proliferation. Therapeutic Effect: In- G
gilteritinib duces apoptosis in mutant-expressing
leukemic cells.
gil-te-ri-ti-nib
(Xospata) PHARMACOKINETICS
j BLACK BOX ALERT j Life- Widely distributed. Metabolized in liver.
threatening and/or fatal differen- Protein binding: 94%. Peak plasma con-
tiation syndrome with symptoms centration: 4–6 hrs. Steady state reached
including fever, dyspnea, hypoxia, in 15 days. Excreted in feces (65%),
pulmonary infiltrates, pleural or
pericardial effusion, rapid weight urine (16%). Half-life: 113 hrs.
gain or peripheral edema, hypoten-
sion, renal dysfunction may occur. LIFESPAN CONSIDERATIONS
Initiate corticosteroid therapy and Pregnancy/Lactation: Avoid preg-
hemodynamic monitoring in pts nancy; may cause fetal harm. Female pts
suspected of differentiation syn-
drome until symptoms resolve. of reproductive potential must use effec-
Do not confuse gilteritinib with tive contraception during treatment and
gefitinib, Gilotrif, or glasdegib. for at least 6 mos after discontinuation.
Unknown if distributed in breast milk.
uCLASSIFICATION Breastfeeding not recommended during
PHARMACOTHERAPEUTIC: FMS-like treatment and for at least 2 mos after
tyrosine kinase 3 (FLT3) inhibitor. discontinuation. Males: Male pts with
Tyrosine kinase inhibitor. CLINICAL: female partners of reproductive potential
Antineoplastic. must use effective contraception during
treatment and for at least 4 mos after
discontinuation. Children: Safety and
USES efficacy not established. Elderly: No age-
Treatment of adults who have relapsed or related precautions noted.
refractory acute myeloid leukemia (AML) INTERACTIONS
with an FMS-like tyrosine kinase 3
(FLT3) mutation. DRUG: Strong CYP3A4 inhibitors
(e.g., clarithromycin, ketoconazole)
PRECAUTIONS may increase concentration/effect.
Contraindications: Hypersensitivity to gil- CYP3A4 inducers used concomitantly
teritinib. Cautions: Baseline neutropenia, with P-gp inducers, strong CYP3A4
hypotension; active infection, cardiac inducers (e.g., carBAMazepine,
disease, hepatic/renal impairment, elec- phenytoin, rifAMPin) may decrease
trolyte imbalance, conditions predispos- concentration/effect. QT interval–pro-
ing to infection (e.g., diabetes, renal longing medications (e.g., amio-
failure, immunocompromised pts, open darone, azithromycin, citalopram,
wounds); pts at risk for QTc interval escitalopram, haloperidol, sotalol)

Canadian trade name Non-Crushable Drug High Alert drug


534 gilteritinib
may increase risk of QTc interval prolon- QTc interval increased by greater
gation. May decrease therapeutic effect than 30 msec on ECG on day 8 of
of selective serotonin receptor in- cycle 1: Confirm with ECG on day 9. If
hibitors (SSRIs) (e.g., escitalopram, confirmed, consider reducing dose to
FLUoxetine, sertraline). HERBAL: St. 80 mg.
John’s wort may decrease concentra-
tion/effect. FOOD: High-fat meals may Other Adverse Reactions
delay absorption. LAB VALUES: May in- Any Grade 3 or higher toxicity:
crease serum alkaline phosphatase, ALT, Withhold treatment until improved to
AST, creatine kinase, triglycerides. May Grade 1, then resume at reduced dose
decrease serum calcium, phosphate, so- of 80 mg.
G dium; neutrophils. Pancreatitis
AVAILABILITY (Rx) Withhold treatment until pancreatitis is
resolved, then resume at reduced dose of
Tablets: 40 mg.
80 mg.
ADMINISTRATION/HANDLING Reversible Posterior Leukoencephalopathy
PO Syndrome
• Give without regard to meals. • Ad- Permanently discontinue.
minister whole; do not break, cut, crush,
or divide tablets. • Tablets cannot be Dosage in Renal Impairment
chewed. • If vomiting occurs after ad- Mild to moderate impairment: No
ministration, give next dose at regularly dose adjustment. Severe impairment:
scheduled time. • If a dose is missed, Not specified; use caution.
administer as soon as possible. • Do
not give a missed dose within 12 hrs of Dosage in Hepatic Impairment
next dose. Mild to moderate impairment: No
dose adjustment. Severe impairment:
INDICATIONS/ROUTES/DOSAGE Not specified; use caution.
Acute Myeloid Leukemia
PO: ADULTS: 120 mg once daily for at SIDE EFFECTS
least 6 mos. Continue until disease pro- Frequent (50%–21%): Myalgia, arthralgia,
gression or unacceptable toxicity. pain (back, bone, chest, extremity, mus-
culoskeletal, neck), asthenia, fatigue,
Dose Modification malaise, fever, mucositis, edema (face,
Based on Common Terminology Criteria generalized, localized, peripheral), rash,
for Adverse Events (CTCAE). diarrhea, dyspnea, nausea, cough, con-
stipation, eye disorder, headache, dizzi-
Differentiation Syndrome ness, hypotension, vomiting. Occasional
Withhold treatment if symptoms are se- (18%–11%): Abdominal pain, neuropathy,
vere and persist for more than 48 hrs insomnia, dysgeusia.
after initiation of corticosteroids. Re-
sume treatment when symptoms improve ADVERSE EFFECTS/TOXIC
to Grade 2 or less. REACTIONS
Life-threatening and/or fatal differentia-
QT Interval Prolongation
tion syndrome, a condition with rapid
QTc interval greater than 500 msec:
proliferation and differentiation of my-
Withhold treatment until QTc interval eloid cells, reported in 3% of pts. Re-
returns to within 30 msec of baseline versible posterior leukoencephalopathy
or 480 msec or less, then resume at re- syndrome reported in 1% of pts. QT in-
duced dose of 80 mg. terval prolongation with QTc interval

underlined – top prescribed drug


gilteritinib 535
greater than 500 msec (1% of pts) and Reversible posterior leukoencephalopa-
QTc interval greater than 60 msec from thy syndrome should be considered in
baseline (7% of pts) have occurred. pts with altered mental status, headache,
Pancreatitis reported in 4% of pts. seizures, visual disturbances. Report ab-
Other significant adverse effects may dominal pain, fever, melena (may indicate
include renal impairment (21% of pts), GI perforation). Monitor daily pattern of
cardiac failure (4% of pts), pericardial bowel activity, stool consistency. Assess
effusion (4% of pts), pericarditis skin for toxic skin reactions, rash. Moni-
(2% of pts), large intestine perforation tor for pancreatitis (severe, steady ab-
(1% of pts). dominal pain often radiating to the back
[with or without vomiting]). Ensure ad-
NURSING CONSIDERATIONS equate hydration, nutrition. G
BASELINE ASSESSMENT PATIENT/FAMILY TEACHING
Obtain CBC, BMP, LFTs, CPK; ECG; preg- • Treatment may depress your immune
nancy test in female pts of reproductive system response and reduce your ability
potential. Replete electrolytes if appli- to fight infection. Report symptoms of
cable. Confirm presence of FLT3-positive infection such as body aches, chills,
mutation. Screen for active infection. cough, fatigue, fever. Avoid those with
Confirm compliance of effective contra- active infection. • Report symptoms of
ception. Question plans of breastfeeding. bone marrow depression such as bruis-
Question history of cardiac/hepatic/renal ing, fatigue, fever, shortness of breath,
disease, GI perforation, pancreatitis. As- weight loss; bleeding easily, bloody urine
sess risk for QT interval prolongation. or stool. • Treatment may cause life-
Receive full medication history and threatening differentiation syndrome as
screen for interactions. Offer emotional early as 2 days after starting therapy. Re-
support. port difficulty breathing, fever, low blood
INTERVENTION/EVALUATION pressure, rapid weight gain, swelling of
the hands or feet, decreased urine out-
Monitor CBC, BMP, LFT, CPK at least wkly put. • Nervous system changes includ-
for 4 wks, then every other week for 4 ing confusion, headache, seizures may
wks, then monthly until discontinuation. indicate life-threatening brain dysfunc-
If QT interval–prolonging medications tion/swelling. • Female pts of child-
cannot be withheld, diligently monitor bearing potential must use effective con-
ECG; serum potassium, magnesium for traception during treatment and up to 2
QT interval prolongation, cardiac arrhyth- mos after last dose. Do not breastfeed. •
mias. An increase of serum creatinine Report liver problems (abdominal pain,
greater than 0.4 mg/dL from baseline may bruising, clay-colored stool, amber- or
indicate renal impairment. Obtain ECG on dark-colored urine, yellowing of the skin
days 8 and 15 of cycle 1 and prior to the or eyes); heart problems (chest tight-
start of next two subsequent cycles. Moni- ness, dizziness, fainting, palpitations,
tor B/P for hypotension, esp. in pts taking shortness of breath skin), kidney prob-
antihypertensives. Monitor for symptoms lems (decreased urine output, flank
of differentiation syndrome (dyspnea, pain, darkened urine); toxic skin reac-
fever hypotension, hypoxia, pulmonary tions (rash, skin eruptions). • Persis-
infiltrates, pleural or pericardial effusion, tent, severe abdominal pain that radiates
rapid weight gain or peripheral edema, to the back (with or without vomiting)
renal dysfunction, or concomitant febrile may indicate acute inflammation of the
neutropenic dermatosis). If differentia- pancreas. • There is a high risk of in-
tion syndrome is suspected, initiate corti- teractions with other medications. Do not
costeroids and hemodynamic monitoring take newly prescribed medications
until symptoms resolve for at least 3 days.
Canadian trade name Non-Crushable Drug High Alert drug
536 glasdegib
unless approved by prescriber who origi- Cautions: Baseline neutropenia, thrombo-
nally started treatment. • Do not take cytopenia; active infection, cardiac dis-
herbal products or ingest grapefruit ease, hepatic/renal impairment, electro-
products. • Report dizziness, chest lyte imbalance; conditions predisposing to
pain, fainting, palpitations, shortness of infection (e.g., diabetes, renal failure, im-
breath); may indicate heart arrhythmia. munocompromised pts, open wounds);
pts at risk for QTc interval prolongation,
cardiac arrhythmias (congenital long QT
syndrome, HF, QT interval–prolonging
glasdegib medications, hypokalemia, hypomagnese-
mia); concomitant use of anticoagulants,
G glas-deg-ib strong CYP3A inhibitors, strong CYP3A
(Daurismo) inducers.
j BLACK BOX ALERT jMay
cause severe birth defects, embryo- ACTION
fetal death in pregnant females. Binds to and inhibits Smoothened (SMO),
Obtain pregnancy test in females the protein involved in Hedgehog signal
of reproductive potential prior to
initiation. Females of reproductive transduction. Therapeutic Effect: Inhib-
potential must use effective contra- its tumor cell growth and reduces the
ception during treatment and for at number of blast cells in marrow.
least 30 days after discontinuation.
Due to potential exposure through PHARMACOKINETICS
semen, males with female partners
of reproductive potential or a Widely distributed. Metabolized in liver.
pregnant partner must use effective Protein binding: 91%. Peak plasma con-
contraception (e.g., condoms) centration: 1.3–1.8 hrs. Steady state
during treatment and for at least 30 reached in 8 days. Excreted in urine
days after discontinuation despite (49%), feces (42%). Half-life: 17.4 hrs.
prior vasectomy.
Do not confuse glasdegib with LIFESPAN CONSIDERATIONS
gefitinib, gilteritinib, sonidegib,
or vismodegib. Pregnancy/Lactation: Avoid preg-
nancy; may cause fetal harm. Female
uCLASSIFICATION pts of reproductive potential must use
PHARMACOTHERAPEUTIC: Hedgehog
effective contraception during treatment
pathway inhibitor. CLINICAL: Antineo- and for at least 30 days after discontinu-
plastic. ation. Unknown if distributed in breast
milk. Breastfeeding not recommended
during treatment and for at least 30 days
USES after discontinuation. Males: May impair
Treatment of newly diagnosed acute my- fertility. Male pts with female partners
eloid leukemia in adults who are 75 yrs of reproductive potential or a pregnant
or older or who have co-morbidities that partner must use effective contraception
preclude use of intensive induction che- (e.g., condoms) during treatment and
motherapy (in combination with low- for at least 30 days after discontinuation
dose cytarabine). despite prior vasectomy. Children: Safety
and efficacy not established. Elderly: No
PRECAUTIONS age-related precautions noted.
b ALERT c Do not donate blood prod- INTERACTIONS
ucts or sperm during treatment and for at
least 30 days after discontinuation. Contra- DRUG: Strong CYP3A4 inhibitors (e.g.,
indications: Hypersensitivity to glasdegib. clarithromycin, ketoconazole) may
increase concentration/effect. Strong

underlined – top prescribed drug


glasdegib 537
CYP3A4 inducers (e.g., carBAM- cytarabine) until improved to Grade 1 or
azepine, phenytoin, rifAMPin) may 0, then resume at same dose or reduce
decrease concentration/effect. QT in- to 50 mg (resume cytarabine at same
terval–prolonging medications dose or reduce to 15 mg or 10 mg). If
(e.g., amiodarone, azithromycin, toxicity recurs, permanently discontinue
haloperidol, sotalol) may increase glasdegib and cytarabine. If recurrent
risk of QT interval prolongation. HERBAL: toxicity is only related to glasdegib,
St. John’s wort may decrease concen- then cytarabine may be continued. Any
tration/effect. FOOD: None known. LAB Grade 3 nonhematologic toxicity:
VALUES: May increase serum alkaline Permanently discontinue glasdegib and
phosphatase, ALT, AST, bilirubin, CPK, cytarabine.
creatinine, potassium. May decrease G
Hgb, neutrophils, platelets; serum cal- QT Interval Prolongation (on at least two
cium, magnesium, phosphate. separate ECGs)
QTc interval 481–500 msec: Assess
AVAILABILITY (Rx) and replete electrolyte levels. Assess and
Tablets: 25 mg, 100 mg. adjust concomitant use of medications
known to cause QTc interval prolonga-
ADMINISTRATION/HANDLING tion. When QTc interval prolongation
PO improves to 480 msec or less, monitor
• Give without regard to meals. • Ad- ECG at least wkly for 2 wks. QTc interval
minister whole; do not break, cut, crush, greater 500 msec: Withhold treatment.
or divide tablets. • Tablets cannot be Assess and replete electrolyte levels. As-
chewed. • If vomiting occurs after ad- sess and adjust concomitant use of medi-
ministration, give next dose at regularly cations known to cause QTc interval pro-
scheduled time. • If a dose is missed, longation. When QTc interval returns to
administer as soon as possible. • Do within 30 msec of baseline or 480 msec
not give a missed dose within 12 hrs of or less, resume at reduced dose of 50
next dose. mg. QTc interval prolongation with
life-threatening arrhythmia: Perma-
INDICATIONS/ROUTES/DOSAGE nently discontinue.
Acute Myeloid Leukemia
Thrombocytopenia
PO: ADULTS, ELDERLY: 100 mg once daily
Platelets less than 10,000 cells/mm3
on days 1–28 (in combination with cy-
for more than 42 days in absence of
tarabine 20 mg SQ twice daily on days
disease: Permanently discontinue glas-
1–10 of each 28-day cycle) for a mini-
mum of 6 cycles. Continue until disease degib and cytarabine.
progression or unacceptable toxicity. Dosage in Renal Impairment
Mild to moderate impairment: No
Dose Modification
Based on Common Terminology Criteria dose adjustment. Severe impairment:
for Adverse Events (CTCAE). Not specified; use caution.
Dosage in Hepatic Impairment
Neutropenia
Mild impairment: No dose adjustment.
Neutrophils less than 500 cells/mm3
Moderate to severe impairment: Not
for more than 42 days in absence of
disease: Permanently discontinue glas-
specified; use caution.
degib and cytarabine. SIDE EFFECTS
Nonhematologic Toxicity Frequent (36%–18%): Fatigue, asthenia,
Any Grade 3 nonhematologic tox- edema, pain (back, bone, chest, mus-
icity: Withhold treatment (including culoskeletal, neck), myalgia, arthralgia,
Canadian trade name Non-Crushable Drug High Alert drug
538 glasdegib
nausea, dyspnea, mucositis, decreased approx. 1 wk after initiation, then monthly
appetite, dysgeusia, rash, constipation, for 2 mos (or more frequently if indi-
pyrexia, diarrhea, cough, vomiting, diz- cated). If QT interval–prolonging medica-
ziness. Occasional (15%–12%): Muscle tions cannot be withheld, diligently moni-
spasm, headache, toothache, alopecia. tor ECG; serum potassium, magnesium for
QT interval prolongation, cardiac arrhyth-
ADVERSE EFFECTS/TOXIC mias. Obtain CK level if muscle aches or
REACTIONS spasms occur. Serum CK level elevations
Anemia, neutropenia, thrombocytopenia usually occur before muscle symptoms
is an expected response to therapy. Car- are reported. Diligently monitor for infec-
diac arrhythmias including atrial fibrilla- tions, febrile neutropenia. Monitor for
G tion, ventricular fibrillation, ventricular bleeding events of any kind; symptoms of
tachycardia may occur. QT interval pro- intracranial bleeding (aphasia, blindness,
longation with QTc interval greater than confusion, facial droop, hemiplegia, sei-
500 msec (5% of pts) and QTc interval zures). Assess skin for toxic skin reac-
greater than 60 msec from baseline (4% tions, rash.
of pts) have occurred. Bleeding events
PATIENT/FAMILY TEACHING
including disseminated intravascular co-
agulation, epistaxis, hemoptysis, hemor- • Treatment may depress your immune
rhage (cerebral, eye, conjunctival, GI, system response and reduce your ability
retinal, tracheal), thrombotic thrombo- to fight infection. Report symptoms of
cytopenic purpura, subdural hematoma infection such as body aches, chills,
reported in 30% of pts. Febrile neutrope- cough, fatigue, fever. Avoid those with
nia reported in 31% of pts. Renal insuf- active infection. • Report symptoms of
ficiency including acute kidney injury, bone marrow depression such as bruis-
oliguria, renal failure reported in 19% of ing, fatigue, fever, shortness of breath,
pts. Infections including pneumonia weight loss; bleeding easily, bloody urine
(19% of pts), sepsis (7% of pts) may or stool. • Do not donate blood or
occurred. blood products during treatment and for
at least 30 days after last dose. • Treat-
NURSING CONSIDERATIONS ment may cause muscle damage, which
may lead to kidney failure. Report mus-
BASELINE ASSESSMENT
culoskeletal symptoms such as muscle
Obtain CBC, BMP, LFTs, CK, ECG; preg- pain/spasms/tenderness/weakness.
nancy test in female pts of reproductive • Report liver problems (abdominal
potential. Replete electrolytes if applica- pain, bruising, clay-colored stool, amber-
ble. Screen for active infection. Confirm or dark-colored urine, yellowing of the
compliance of effective contraception. skin or eyes), hemorrhagic stroke (con-
Receive full medication history and fusion, difficulty speaking, one-sided
screen for interactions. Assess risk for weakness or paralysis, loss of vision),
QT interval prolongation. Question his- kidney problems (decreased urine out-
tory of cardiac/pulmonary/renal disease, put, flank pain, darkened urine), skin
cardiac arrhythmias. Offer emotional reactions (rash, skin eruptions), bleed-
support. ing of any kind. • Report dizziness,
INTERVENTION/EVALUATION chest pain, fainting, palpitations, short-
ness of breath); may indicate heart ar-
Monitor CBC, BMP, LFTs at least wkly for 1 rhythmia. • Female pts and male pts
mo, then monitor electrolytes, BUN, se- with female partners of childbearing po-
rum creatinine, GFR, CrCl monthly there- tential must use effective contraception
after. An increase of serum creatinine during treatment and up to 30 days after
greater than 0.4 mg/dL from baseline may last dose. Do not breastfeed. Male pts
indicate renal impairment. Obtain ECG
underlined – top prescribed drug
glatiramer 539
must use condoms during sexual activity LIFESPAN CONSIDERATIONS
during treatment and up to 30 days after Pregnancy/Lactation: Unknown if
last dose. • There is a high risk of in- distributed in breast milk. Children/El-
teractions with other medications. Do not derly: Safety and efficacy not established.
take newly prescribed medications un-
less approved by prescriber who origi- INTERACTIONS
nally started treatment. • Avoid grape- DRUG: May decrease therapeutic effect of
fruit products, herbal supplements (esp. BCG (intravesical), vaccines (live).
St. John’s wort). May increase toxic/adverse effects of live
vaccines. HERBAL: Echinacea may de-
crease effects. FOOD: None known. LAB
G
VALUES: None significant.
glatiramer
AVAILABILITY (Rx)
gla-tir-a-mer Injection Solution: (Copaxone, Glatopa):
(Copaxone, Glatopa, Glatect ) 20 mg/mL in prefilled syringes, 40 mg/
Do not confuse Copaxone with mL in prefilled syringes.
Compazine.
ADMINISTRATION/HANDLING
uCLASSIFICATION
SQ
PHARMACOTHERAPEUTIC: Immu-
• Refrigerate syringes (bring to room
nosuppressive. CLINICAL: Neurolog- temperature before use). • May be
ic agent for multiple sclerosis. stored at room temperature for up to 1
mo. • Avoid heat, intense light. •
USES Inject into deltoid region, abdomen,
gluteus maximus, or lateral aspect
­
Treatment of relapsing, remitting mul- of thigh. • Prefilled syringe suitable
tiple sclerosis. for single use only; discard unused
PRECAUTIONS ­portions.
Contraindications: Hypersensitivity to INDICATIONS/ROUTES/DOSAGE
glatiramer, mannitol. Cautions: Pts ex- Multiple Sclerosis
hibiting immediate postinjection reaction Note: Dose forms 20 mg/mL and 40 mg/
(flushing, chest pain, palpitations, anxi- mL are not interchangeable.
ety, dyspnea, urticaria). SQ: ADULTS, ELDERLY: 20 mg once daily
ACTION or 40 mg 3 times/wk at least 48 hrs apart.
Induces/activates T-lymphocyte suppres- Dosage in Renal/Hepatic Impairment
sor cells specific to myelin antigens. May No dose adjustment.
also interfere with the antigen-presenting
function of immune cells. Therapeutic SIDE EFFECTS
Effect: Slows progression of multiple Expected (73%–40%): Pain, erythema,
sclerosis. inflammation, pruritus at injection site,
asthenia. Frequent (27%–18%): Arthral-
PHARMACOKINETICS gia, vasodilation, anxiety, hypertonia,
Substantial fraction of glatiramer is hy- nausea, transient chest pain, dyspnea,
drolyzed locally. Some fraction of injected flu-like symptoms, rash, pruritus. Oc-
material enters lymphatic circulation, casional (17%–10%): Palpitations, back
reaching regional lymph nodes; some pain, diaphoresis, rhinitis, diarrhea,
may enter systemic circulation intact. urinary urgency. Rare (less than 9%): An-

Canadian trade name Non-Crushable Drug High Alert drug


540 glecaprevir/­pibrentasvir
orexia, fever, neck pain, peripheral fosamprenavir, paritaprevir,
edema, ear pain, facial edema, vertigo, simeprevir, telaprevir, or voxil-
vomiting. aprevir, or pibrentasvir with da-
clatasvir, ledipasvir, ombitasvir,
ADVERSE EFFECTS/TOXIC or velpatasvir.
REACTIONS
Infection occurs commonly. Lymphade- FIXED-COMBINATION(S)
nopathy occurs occasionally. Mavyret: glecaprevir/pibrentasvir:
100 mg/40 mg.
NURSING CONSIDERATIONS
uCLASSIFICATION
BASELINE ASSESSMENT
G PHARMACOTHERAPEUTIC: NS3/4A
Assess baseline muscle strength, gait, protease inhibitor, NS5A protein in-
voice quality, pain level; ability to con- hibitor. CLINICAL: Antihepaciviral.
duct activities of daily living. Question
other baseline symptoms including
bowel/bladder dysfunction, depres- USES
sion, dizziness, fatigue, paresthesia, Treatment of adults and pediatric pts 12 yrs
spasticity, sexual dysfunction, trem- and older or weighing 45 kg or more with
ors. chronic hepatitis C virus (HCV) infection
INTERVENTION/EVALUATION without cirrhosis or with compensated cir-
Observe injection site for reaction. Moni- rhosis who have genotype 1, 2, 3, 4, 5, or 6
tor for fever, chills (evidence of infec- infection. Treatment of adults and pediatric
tion). Observe for improvement of symp- pts 12 yrs and older or weighing 45 kg or
toms, neurologic function. more with HCV genotype 1 infection who
have previously been treated with an HCV
PATIENT/FAMILY TEACHING regimen containing an NS5A inhibitor or an
• Report difficulty in breathing/swallow- NS5A protease inhibitor, but not both.
ing, rash, itching, swelling of lower ex-
tremities, fatigue. • Avoid pregnancy. PRECAUTIONS
Contraindications: Hypersensitivity to gle-
caprevir, pibrentasvir. Concomitant use
with atazanavir, rifampin. Severe hepatic
glecaprevir/­ impairment. Cautions: HIV infection, he-
patic disease unrelated to HCV infection,
pibrentasvir HBV infection. Concomitant use of P-gp
substrates or inhibitors, BCRP substrates,
glec-a-pre-vir/pi-brent-as-vir CYP3A4 inducers. Not recommended in
(Mavyret) pts with moderate hepatic impairment.
j BLACK BOX ALERT j Test all ACTION
pts for hepatitis B virus (HBV) infec-
tion before initiation. HBV reactiva- Glecaprevir inhibits NS3/4A protease,
tion was reported in HCV/HBV co- necessary for proteolytic cleavage of
infected pts who were undergoing HCV-encoded polyprotein. Pibrentasvir
or had completed treatment with
HCV direct-acting antivirals and inhibits the HCV NS5A protein, essential
were not receiving HBV antiviral for viral replication. Therapeutic Ef-
therapy. HBV reactivation may fect: Inhibits viral replication of HCV.
cause fulminant hepatitis, hepatic
failure, and death. PHARMACOKINETICS
Do not confuse glecaprevir Widely distributed. Glecaprevir metabo-
with boceprevir, grazoprevir, lized in liver. Pibrentasvir metabolism not

underlined – top prescribed drug


glecaprevir/­pibrentasvir 541
specified. Protein binding: (glecaprevir): Treatment Regimen and Duration
98%; (pibrentasvir): greater than 99%. Treatment-Naïve HCV Genotype 1, 2, 3,
Peak plasma concentration: 5 hrs. Gle- 4, 5, or 6
caprevir excreted in feces (92%), urine Without cirrhosis: glecaprevir/pibrentas-
(1%). Pibrentasvir primarily excreted in vir for 8 wks. With compensated cirrho-
feces (97%). Half-life: (glecaprevir): 6 sis: glecaprevir/pibrentasvir for 12 wks.
hrs; (pibrentasvir): 13 hrs.
Treatment-Experienced Genotype 1
LIFESPAN CONSIDERATIONS Prior treatment with NS5A inhibitor
Pregnancy/Lactation: Unknown if dis- (without NS3/4A protease inhibitor)
tributed in breast milk. Children: Safety without cirrhosis or with compen-
and efficacy not established. Elderly: No sated cirrhosis: glecaprevir/pibrentas- G
age-related precautions noted. vir for 16 wks. Prior treatment with
NS3/4A protease inhibitor (without
INTERACTIONS NS5A inhibitor) without cirrhosis or
DRUG: Atazanavir, cycloSPORINE, with compensated cirrhosis: glecap-
darunavir, efavirenz, irinotecan may revir/pibrentasvir for 12 wks. Prior treat-
increase concentration of glecaprevir/ ment with peginterferon, ribavirin,
pibrentasvir. Glecaprevir/pibrentasvir sofosbuvir without cirrhosis: glecap-
may increase concentration of afatinib, revir/pibrentasvir for 8 wks. Prior treat-
atorvastatin, digoxin, lovastatin, ment with peginterferon, ribavirin,
simvastatin, topotecan, venetoclax, sofosbuvir with compensated cirrho-
voxilaprevir. CYP3A4 inducers sis: glecaprevir/pibrentasvir for 12 wks.
(e.g., carBAMazepine, phenytoin, Treatment-Experienced Genotype 2, 4, 5, or 6
rifAMPin) may decrease concentra- Prior treatment with peginterferon,
tion/effect. Ethinyl estradiol–con- ribavirin, sofosbuvir without cirrho-
taining hormonal contraceptives sis: glecaprevir/pibrentasvir for 8 wks.
may increase risk of hepatotoxicity. Prior treatment with peginterferon,
HERBAL: St. John’s wort may decrease ribavirin, sofosbuvir with compen-
concentration/effect. FOOD: None sated cirrhosis: glecaprevir/pibrentas-
known. LAB VALUES: May increase se- vir for 12 wks.
rum bilirubin.
Treatment-Experienced Genotype 3
AVAILABILITY (Rx) Prior treatment with peginterferon,
Fixed-Dose Combination Tablets: glecap- ribavirin, sofosbuvir without cirrhosis
revir/pibrentasvir: 100 mg/40 mg. or with compensated cirrhosis: gleca-
previr/pibrentasvir for 16 wks.
ADMINISTRATION/HANDLING
Liver/Kidney Transplant Recipients
PO Recommend glecaprevir/pibrentasvir for
• Give with food. • If dose is missed, 12 wks. A treatment duration of 16 wks is
administer as soon as possible if no more recommended in pts with HCV genotype
than 18 hrs have passed since the last 1 who are treatment-experienced (prior
dose. If more than 18 hrs have passed, treatment with NS5A inhibitor [without
skip the missed dose and administer the NS3/4A protease inhibitor]) or in pts
next dose at regularly scheduled time. with HCV genotype 3 who are treatment-
INDICATIONS/ROUTES/DOSAGE experienced (prior treatment with pegin-
terferon, ribavirin, sofosbuvir).
Hepatitis C Virus Infection
PO: ADULTS, ELDERLY: 3 tablets once Dosage in Renal Impairment
daily (total dose: glecaprevir 300 mg and Mild to severe impairment: No dose
pibrentasvir 120 mg). adjustment.
Canadian trade name Non-Crushable Drug High Alert drug
542 glimepiride
Dosage in Hepatic Impairment cause kidney failure. Report flank pain,
Mild impairment: No dose adjustment. muscle pain, darkened urine, decreased
Moderate impairment: Not recom- urinary output. • Ethinyl estradiol–
mended. Severe impairment: Contra- containing hormonal contraceptives may
indicated. increase risk of liver injury and are not
recommended.
SIDE EFFECTS
Frequent (16%–11%): Headache, fatigue.
Occasional (9%–7%): Nausea, diarrhea,
pruritus. glimepiride
G ADVERSE EFFECTS/TOXIC glye-mep-ir-ide
REACTIONS (Amaryl)
HBV reactivation was reported in pts co- Do not confuse Amaryl with
infected with HBV/HVC. HBV reactivation Altace, Amerge, or Reminyl,
may result in fulminant hepatitis, hepatic or Avandaryl with Benadryl,
failure, death. or glimepiride with glipiZIDE
or glyBURIDE.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
FIXED-COMBINATION(S)
Obtain LFT, HCV-RNA level. Confirm hepati- Avandaryl: glimepiride/rosiglitazone
tis C virus genotype. Test all pts for hepatitis (an antidiabetic): 1 mg/4 mg, 2 mg/4
B virus infection. Initiate anti-HBV therapy mg, 4 mg/4 mg.
if warranted. Question history of hepatic Duetact: glimepiride/pioglitazone (an
disease unrelated to HCV infection, HIV antidiabetic): 2 mg/30 mg, 4 mg/30 mg.
infection; liver/kidney transplantation; con- uCLASSIFICATION
comitant use of other antiretroviral therapy.
PHARMACOTHERAPEUTIC: Sulfonyl-
Receive full medication history and screen
for interactions (esp. atazanavir, rifampin). urea. CLINICAL: Antidiabetic agent.

INTERVENTION/EVALUATION
USES
Periodically monitor HCV-RNA level
for treatment effectiveness (or upon Adjunct to diet, exercise in the manage-
completion of treatment). Closely moni- ment of type 2 diabetes mellitus.
tor for exacerbation of hepatitis or HBV
PRECAUTIONS
reactivation. Monitor for rhabdomyolysis
(muscle weakness, myalgia, myopathy, Contraindications: Hypersensitivity to
decreased urinary output) in pts taking glimepiride, sulfonamides. Diabetic keto-
HMG-CoA reductase inhibitors. acidosis (with or without coma). Cautions:
Renal/hepatic impairment, glucose-altering
PATIENT/FAMILY TEACHING conditions (fever, trauma, infection),
• Take with food. • There is a high G6PD deficiency, elderly, malnourished.
risk of drug interactions with other med- Allergy to sulfa.
ications. Do not take newly prescribed
medications unless approved by pre- ACTION
scriber who originally started treatment. Stimulates release of insulin from beta
Do not take herbal products. • Pts tak- cells of pancreas, decreases glucose
ing statins (lipid medication) may have output from liver, increases insulin sen-
an increased risk of rhabdomyolysis, a sitivity at peripheral sites. Therapeutic
breakdown of muscle tissue that can Effect: Lowers serum glucose.

underlined – top prescribed drug


glimepiride 543

PHARMACOKINETICS Dosage in Renal Impairment


Route Onset Peak Duration
Initially, 1 mg/day, then titrate dose based
on fasting serum glucose levels.
PO N/A 2–3 hrs 24 hrs
Dosage in Hepatic Impairment
Completely absorbed from GI tract. Pro-
No dose adjustment (not studied).
tein binding: greater than 99%. Metabo-
lized in liver. Excreted in urine (60%), SIDE EFFECTS
feces (40%). Half-life: 5–9.2 hrs.
Rare (less than 3%): Altered taste, dizzi-
LIFESPAN CONSIDERATIONS ness, drowsiness, weight gain, constipation,
diarrhea, heartburn, nausea, vomiting,
Pregnancy/Lactation: Avoid preg-
stomach fullness, headache, photosensitiv- G
nancy. Unknown if distributed in breast
ity, peeling of skin, pruritus, rash.
milk. Children: Safety and efficacy not
established. Elderly: Hypoglycemia may ADVERSE EFFECTS/TOXIC
be difficult to recognize. Age-related re- REACTIONS
nal impairment may increase sensitivity
Overdose or insufficient food intake
to glucose-lowering effect.
may produce hypoglycemia (esp. with
INTERACTIONS increased glucose demands). GI hem-
orrhage, cholestatic hepatic jaundice,
DRUG: Beta blockers (e.g., carvedilol,
leukopenia, thrombocytopenia, pancyto-
metoprolol) may increase hypoglycemic
penia, agranulocytosis, aplastic or hemo-
effect, mask signs of hypoglycemia. Cimeti-
lytic anemia occur rarely.
dine, ciprofloxacin, fluconazole, ra-
NITIdine, large doses of salicylates may NURSING CONSIDERATIONS
increase effect. RifAMPin may decrease
concentration/effect. Thiazolidinediones BASELINE ASSESSMENT
(e.g., pioglitazone) may increase hypo- Check serum glucose level. Discuss
glycemic effect. HERBAL: Herbals with lifestyle to determine extent of learn-
hypoglycemic properties (e.g., fenu- ing, emotional needs. Ensure follow-up
greek) may increase risk of hypoglycemia. instruction if pt or family does not thor-
FOOD: Alcohol may cause rare disulfiram oughly understand diabetes management
reaction. LAB VALUES: May increase LDH or serum glucose testing technique.
concentrations, serum alkaline phospha-
tase, ALT, AST, bilirubin, C-peptide. INTERVENTION/EVALUATION
Monitor serum glucose level, food in-
AVAILABILITY (Rx) take. Assess for hypoglycemia (cool/wet
Tablets: 1 mg, 2 mg, 4 mg. skin, tremors, dizziness, anxiety, head-
ache, tachycardia, perioral numbness,
ADMINISTRATION/HANDLING hunger, diplopia), hyperglycemia (poly-
PO uria, polyphagia, polydipsia, nausea,
• Give with breakfast or first main meal. vomiting, dim vision, fatigue, deep or
rapid breathing). Be alert to conditions
INDICATIONS/ROUTES/DOSAGE that alter glucose requirements (fever,
Diabetes Mellitus increased activity or stress, trauma, sur-
PO: ADULTS: Initially, 1–2 mg once gical procedure).
daily with breakfast or first main meal. PATIENT/ FAMILY TEACHING
May increase by 1–2 mg q1–2wks,
based on serum glucose response. • Diet and exercise are principal parts of
Maximum: 8 mg/day. ELDERLY: Ini- treatment; do not skip or delay meals. •
tially, 1 mg/day. Titrate dose to avoid Avoid alcohol. • Carry candy, sugar pack-
hypoglycemia. ets, other quick-acting sugar supplements for

Canadian trade name Non-Crushable Drug High Alert drug


544 glipiZIDE
immediate response to hypoglycemia. PHARMACOKINETICS
• Wear medical alert identification. Route Onset Peak Duration
• Check with physician when glucose de- PO 15–30 2–3 hrs 12–24 hrs
mands are altered (fever, infection, trauma, min
stress, heavy physical activity). • Avoid Extended- 2–3 hrs 6–12 hrs 24 hrs
direct exposure to sunlight. release

Well absorbed from GI tract. Pro-


tein binding: 92%–99%. Metabolized
glipiZIDE in liver. Excreted in urine. Half-
life: 2–4 hrs.
G glip-i-zide
(Glucotrol, Glucotrol XL) LIFESPAN CONSIDERATIONS
Do not confuse glipiZIDE with Pregnancy/Lactation: Agents other
glimepiride or glyBURIDE, or than glipizide are recommended to
Glucotrol with Glucophage or treat diabetes in pregnant women. Glipi-
Glucotrol XL. ZIDE given within 1 mo of delivery may
produce neonatal hypoglycemia. Drug
FIXED-COMBINATION(S) crosses placenta. Distributed in breast
GlipiZIDE/metFORMIN (an antidia- milk. Children: Safety and efficacy not
betic): 2.5 mg/250 mg, 2.5 mg/500 established. Elderly: Hypoglycemia may
mg, 5 mg/500 mg. be difficult to recognize. Age-related re-
nal impairment may increase sensitivity
uCLASSIFICATION to glucose-lowering effect.
PHARMACOTHERAPEUTIC: Sulfony-
lurea. CLINICAL: Antidiabetic agent. INTERACTIONS
DRUG: Beta blockers (e.g., carvedilol,
metoprolol) may increase hypoglyce-
USES mic effect, mask signs of hypoglycemia.
Adjunct to diet, exercise in management RifAMPin may decrease concentration/
of type 2 diabetes mellitus. effect. Thiazolidinediones (e.g., pio-
glitazone) may increase hypoglycemic
PRECAUTIONS effect. HERBAL: Herbals with hypogly-
Contraindications: Hypersensitivity to cemic properties (e.g., fenugreek)
glipiZIDE, sulfonamides. Diabetic ke- may increase risk of hypoglycemia.
toacidosis with or without coma, type FOOD: None known. LAB VALUES: May
1 diabetes mellitus. Cautions: Elderly, increase serum alkaline phosphatase,
malnourished, concomitant use of beta LDH, ALT, AST, bilirubin, C-peptide.
blockers, pts with G6PD deficiency, he-
patic/renal impairment. Avoid use of AVAILABILITY (Rx)
extended-release tablets in pts with stric- Tablets: 5 mg, 10 mg. Tablets: (Extended-
ture/narrowing of GI tract. Release): 2.5 mg, 5 mg, 10 mg.

ACTION ADMINISTRATION/HANDLING
Stimulates release of insulin from beta PO
cells of pancreas, decreases glucose • Give immediate-release tablets 30 min
output from liver, increases insulin sen- before meals. Give extended-release tablets
sitivity at peripheral sites. Therapeutic with breakfast. • Do not crush, cut, dis-
Effect: Lowers serum glucose. solve, or divide extended-release tablets.

underlined – top prescribed drug


glyBURIDE 545

INDICATIONS/ROUTES/DOSAGE INTERVENTION/EVALUATION
Diabetes Mellitus Monitor serum glucose level, food in-
PO: ADULTS: (Immediate-Release): take. Assess for hypoglycemia (cool/wet
Initially, 2.5 mg/day. Adjust dosage in 2.5- skin, tremors, dizziness, anxiety, head-
to 5-mg increments at intervals of 1–2 wks. ache, tachycardia, perioral numbness,
Maximum effective dose: 20 mg/day. hunger, diplopia), hyperglycemia (poly-
(Extended-Release): Initially, 2.5–5 mg/ uria, polyphagia, polydipsia, nausea,
day. May increase dose no more frequently vomiting, dim vision, fatigue, deep or
than q7days. Maximum dose: 20 mg/day. rapid breathing). Be alert to conditions
ELDERLY: (Immediate-Release): Ini- that alter glucose requirements (fever,
tially, 2.5 mg/day. May increase by 2.5–5 increased activity or stress, trauma, sur-
mg/day q1–2wks. Maintenance dose gical procedure). G
should be conservative to avoid hypoglyce- PATIENT/ FAMILY TEACHING
mia. (Extended-Release): Initially, 2.5
mg/day. Maintenance dose should be con- • Diet and exercise are principal parts of
servative to avoid hypoglycemia. treatment; do not skip or delay
meals. • Avoid alcohol. • Carry candy,
Dosage in Renal Impairment sugar packets, other quick-acting sugar
For creatinine clearance of 50 mL/min or supplements for immediate response to
less, reduce dose by 50%. hypoglycemia. • Wear medical alert
identification. • Check with physician
Dosage in Hepatic Impairment when glucose demands are altered (fever,
(Immediate-Release): Initial dose: 2.5 infection, trauma, stress, heavy physical
mg/day. activity). • Avoid direct exposure to
sunlight.
SIDE EFFECTS
Rare (less than 3%): Altered taste,
d­ izziness, drowsiness, weight gain, con-
stipation, diarrhea, heartburn, nausea,
vomiting, headache, photosensitivity, glyBURIDE
peeling of skin, pruritus, rash.
glye-bue-ride
ADVERSE EFFECTS/TOXIC (DiaBeta , Euglucon , Glynase)
REACTIONS Do not confuse DiaBeta with
Overdose or insufficient food intake may Zebeta, glyBURIDE with glime-
produce hypoglycemia (esp. with increased piride, glipiZIDE, or Glucotrol.
glucose demands). GI hemorrhage, chole- FIXED-COMBINATION(S)
static hepatic jaundice, leukopenia, throm-
bocytopenia, pancytopenia, agranulocytosis, Glucovance: glyBURIDE/metFORMIN
aplastic or hemolytic anemia occur rarely. (an antidiabetic): 1.25 mg/250 mg,
2.5 mg/500 mg, 5 mg/500 mg.
NURSING CONSIDERATIONS
uCLASSIFICATION
BASELINE ASSESSMENT PHARMACOTHERAPEUTIC: Sulfonyl-
Check serum glucose level. Discuss urea. CLINICAL: Antidiabetic agent.
lifestyle to determine extent of learn-
ing, emotional needs. Ensure follow-
up instruction if pt or family does USES
not thoroughly understand diabetes Adjunct to diet, exercise in management
management or serum glucose testing of stable, mild to moderately severe type
technique. 2 diabetes mellitus.

Canadian trade name Non-Crushable Drug High Alert drug


546 glyBURIDE

PRECAUTIONS AVAILABILITY (Rx)


Contraindications: Hypersensitivity to Tablets: 1.25 mg, 2.5 mg, 5 mg. Tablets,
glyBURIDE. Diabetic ketoacidosis with Micronized: 1.5 mg, 3 mg, 6 mg.
or without coma, type 1 diabetes mel-
litus, concurrent use with bosentan. ADMINISTRATION/HANDLING
Cautions: Stress, elderly, debilitated pts, PO
malnourished, severe hepatic/renal im- • May give with food at same time each
pairment, G6PD deficiency, adrenal and/ day.
or pituitary insufficiency.
INDICATIONS/ROUTES/DOSAGE
ACTION Diabetes Mellitus
G Stimulates release of insulin from beta PO: (Tablets): ADULTS: Initially, 1.25–5
cells of pancreas, decreases glucose mg. May increase by 2.5 mg/day at wkly
output from liver, increases insulin sen- intervals. Maintenance: 1.25–20 mg/
sitivity at peripheral sites. Therapeutic day as single or divided doses. Maxi-
Effect: Lowers serum glucose level. mum: 20 mg/day. ELDERLY: Initially, 1.25
mg daily. Conservative initial and mainte-
PHARMACOKINETICS nance doses are recommended to avoid
Route Onset Peak Duration hypoglycemic reactions.
PO 0.25–1 hr 1–2 hrs 12–24 hrs PO: (Tablets, Micronized): ADULTS:
Initially 0.75–3 mg/day. May increase by
Well absorbed from GI tract. Protein 1.5 mg/day at wkly intervals. Mainte-
binding: 99%. Metabolized in liver. Pri- nance: 0.75–12 mg/day as a single dose or
marily excreted in urine. Not removed by in divided doses. Maximum: 12 mg/day.
hemodialysis. Half-life: 5–16 hrs. ELDERLY: Initially, 0.75 mg daily. Conser-
vative initial and maintenance doses are
LIFESPAN CONSIDERATIONS recommended to avoid hypoglycemic
Pregnancy/Lactation: Crosses pla- reactions.
centa. Distributed in breast milk. May
produce neonatal hypoglycemia if Dosage in Renal Impairment
given within 2 wks of delivery. Chil- Not recommended for pts with creatinine
dren: Safety and efficacy not estab- clearance less than 60 mL/min.
lished. Elderly: Hypoglycemia may be
difficult to recognize. Age-related renal Dosage in Hepatic Impairment
impairment may increase sensitivity to No dose adjustment.
glucose-lowering effect. SIDE EFFECTS
INTERACTIONS Rare (less than 3%): Altered taste, dizzi-
DRUG: Beta blockers (e.g., carvedilol, ness, drowsiness, weight gain, constipa-
metoprolol) may increase hypoglyce- tion, diarrhea, heartburn, nausea, vomit-
mic effect, mask signs of hypoglycemia. ing, headache, photosensitivity, peeling of
RifAMPin may decrease concentration/ skin, pruritus, rash.
effect. Thiazolidinediones (e.g., pio- ADVERSE EFFECTS/TOXIC
glitazone) may increase hypoglycemic REACTIONS
effect. HERBAL: Herbals with hypogly-
cemic properties (e.g., fenugreek) Overdose or insufficient food intake may
may increase risk of hypoglycemia. produce hypoglycemia (esp. in pts with
FOOD: None known. LAB VALUES: May increased glucose demands). Cholestatic
increase serum alkaline phosphatase, jaundice, leukopenia, thrombocytopenia,
LDH, ALT, AST, bilirubin, C-peptide. pancytopenia, agranulocytosis, aplastic
or hemolytic anemia occur rarely.

underlined – top prescribed drug


golimumab 547

NURSING CONSIDERATIONS uCLASSIFICATION


PHARMACOTHERAPEUTIC: Mono-
BASELINE ASSESSMENT clonal antibody. Tumor necrosis
Check serum glucose level. Discuss factor (TNF) blocking agent. CLINI-
lifestyle to determine extent of learn- CAL: Antipsoriatic agent, antirheu-
ing, emotional needs. Ensure follow-up matic, disease-modifying agent.
instruction if pt or family does not thor-
oughly understand diabetes management
or glucose testing technique. USES
INTERVENTION/EVALUATION
Simponi, Simponi Aria: Used alone
or in combination with methotrexate
Monitor serum glucose level, food intake. for the treatment of adult pts with active G
Assess for hypoglycemia (cool/wet skin, psoriatic arthritis. Used in combination
tremors, dizziness, anxiety, headache, with methotrexate for the treatment of
tachycardia, perioral numbness, hunger, adult pts with moderately to severely ac-
diplopia); hyperglycemia (polyuria, poly- tive rheumatoid arthritis. Used alone or
phagia, polydipsia, nausea, vomiting, dim in combination with methotrexate for
vision, fatigue, deep or rapid breathing). the treatment of adult pts with active
Be alert to conditions that alter glucose ankylosing spondylitis. Simponi: (Ad-
requirements (fever, increased activity or ditional) Treatment of moderate to se-
stress, trauma, surgical procedure). vere active ulcerative colitis in pts with
PATIENT/ FAMILY TEACHING corticosteroid dependence or who are
• Diet and exercise are principal parts refractory/intolerant to aminosalicylates,
of treatment; do not skip or delay oral steroids, azathioprine, or 6-mercap-
meals. • Avoid alcohol. • Carry candy, topurine.
sugar packets, other quick-acting sugar PRECAUTIONS
supplements for immediate response to
Contraindications: Hypersensitivity to
hypoglycemia. • Wear medical alert
identification. • Check with physician golimumab. Cautions: Elderly, concomi-
when glucose demands are altered (fe- tant immunosuppressants, co-morbid
ver, infection, trauma, stress, heavy phys- conditions predisposing to infections
ical activity). • Avoid direct exposure to (e.g., diabetes). Residence or travel from
sunlight. areas of endemic mycosis; tuberculosis,
underlying hematologic disorders, pre-
existing or recent-onset demyelinating
golimumab disorders (e.g., multiple sclerosis, poly-
neuropathy), pts with HF or decreased
goe-lim-ue-mab left ventricular function. Avoid concomi-
(Simponi, Simponi Aria) tant use with live vaccines, abatacept, or
anakinra (increased incidence of serious
j BLACK BOX ALERT j Tubercu- infections). Do not start during an active
losis (TB), invasive fungal infections,
other opportunistic infections infection.
reported. Discontinue treatment if
active infection or sepsis occurs. ACTION
Test for TB prior to and during treat- Binds specifically to tumor necrosis factor
ment, regardless of initial result; if
positive, start treatment for TB prior (TNF) alpha, blocking its interaction with
to initiating therapy. Lymphoma, other cell surface TNF receptors. Therapeu-
malignancies reported in pts treated tic Effect: Alters biologic activity of TNF
with tumor necrosis factor blockers. alpha, reduces inflammation, may alter
Do not confuse Simponi (SQ) pathophysiology of rheumatoid arthritis.
with Simponi Aria (IV)
Canadian trade name Non-Crushable Drug High Alert drug
548 golimumab

PHARMACOKINETICS not pull autoinjector away from skin until


Serum concentration reaches steady state a first “click” sound is heard and then a
by wk 12. Elimination pathway not speci- second “click” sound (injection is fin-
fied. Half-life: 12–14 days. ished and needle is pulled back). This
usually takes 3 to 6 sec but may take up
LIFESPAN CONSIDERATIONS to 15 sec for the second “click” to be
Pregnancy/Lactation: Unknown if heard. If autoinjector is pulled away from
distributed in breast milk. Must either skin before injection is completed, full
discontinue drug or discontinue breast- dose may not be administered.
feeding. Children: Safety and efficacy Prefilled Syringe
not established. Elderly: May have in- • Gently pinch skin and hold firmly. Use
G creased risk of serious infections, ma- a quick, dart-like motion to insert needle
lignancy. into pinched skin at a 45-degree angle.
Storage • Refrigerate; do not freeze.
INTERACTIONS Do not shake. • Solution appears slightly
DRUG: Anakinra, anti-TNF agents, opalescent, colorless to light yellow. Dis-
baricitinib, pimecrolimus, riTUX- card if cloudy or contains particulate.
imab, tacrolimus (topical), tocili-
zumab may increase adverse effects. May Simponi Aria
decrease therapeutic effect of BCG (intra- b ALERT c Use in-line 0.22-micron fil-
vesical), vaccines (live). May increase ter.
levels, adverse effects of belimumab,
IV
natalizumab, tofacitinib, vaccines
(live). HERBAL: Echinacea may decrease Reconstitution • Calculate dosage
effects. FOOD: None known. LAB VAL- and number of vials needed based on pt
UES: May increase ALT, AST. May decrease weight. • Visually inspect for particu-
Hgb, leukocytes, neutrophils, platelets. late matter. • Dilute in 100 mL 0.9%
NaCl. • Prior to mixing, withdraw and
AVAILABILITY (Rx) discard volume of 0.9% NaCl equal to the
Injection Solution: (Simponi): 50 mg/0.5 volume of patient-dosed solution. •
mL, 100 mg/mL in single-dose prefilled Slowly inject solution into bag and gently
autoinjector or prefilled syringe. Injec- mix. • Do not shake.
tion Solution: (Simponi Aria): 50 mg/4 mL Rate of administration • Infuse over
per single-use vial (12.5 mg/mL). 30 min using an in-line low protein-
binding 0.22-micron filter.
ADMINISTRATION/HANDLING Storage • Refrigerate vials, prefilled
Simponi SQ syringes • Vial solution should be col-
• Remove prefilled syringe or autoinjec- orless to light yellow and opales-
tor from refrigerator. Allow to sit at room cent. • It is normal for solution to de-
temperature for 30 min; do not warm in velop fine translucent particles since
any other way. • Avoid areas where skin drug is a protein. • Do not use if
is scarred, tender, bruised, red, scaly, opaque particles, discoloration, or other
hard. Recommended injection site is foreign particles are present. • May
front of middle thighs, although lower store diluted solution at room tempera-
abdomen 2 inches below navel or outer, ture up to 4 hrs.
upper arms are acceptable. • Inject
within 5 min after cap has been removed. IV INCOMPATIBILITIES
Autoinjector
• Push open end of autoinjector firmly Do not infuse concomitantly with other
against skin at 90-degree angle. • Do drugs.

underlined – top prescribed drug


golimumab 549

INDICATIONS/ROUTES/DOSAGE noma, new malignancies. New onset or


Active Psoriatic Arthritis exacerbation of CNS demyelinating dis-
Note: Use alone or in combination orders, including multiple sclerosis, or
with methotrexate or other nonbiologic worsening of HF have occurred. Viral
DMARD. SQ: (Simponi): ADULTS, EL- reactivation of herpes zoster, HIV, hepa-
DERLY: 50 mg once monthly. titis B virus infection may occur. Pts who
IV infusion: (Simponi Aria): ADULTS, receive TNF blockers have risk of auto-
ELDERLY: 2 mg/kg at wk 0, 4 then q8wks antibody formation (immunogenicity).
thereafter. Hypersensitivity reactions including ana-
phylaxis reported. May induce lupus-like
Moderate to Severe Active Rheumatoid symptoms (butterfly rash, new joint pain,
Arthritis (with methotrexate) peripheral edema, UV sensitivity). G
SQ: (Simponi): ADULTS, ELDERLY: 50
mg once monthly. NURSING CONSIDERATIONS
IV infusion: (Simponi Aria): ADULTS, BASELINE ASSESSMENT
ELDERLY: 2 mg/kg at wk 0 and wk 4.
Obtain baseline LFT, CBC, vital signs, urine
Then, decrease frequency to q8wks.
pregnancy. Obtain B-type natriuretic pep-
Active Ankylosing Spondylitis tide (BNP) level and review echocardio-
Note: Use alone or in combination gram in pts with history of HF. Do not ini-
with methotrexate or other nonbiologic tiate therapy if active infection suspected.
DMARD. SQ: (Simponi): ADULTS, EL- Evaluate for active TB and test for latent
DERLY: 50 mg once monthly. infection prior to and during treatment.
IV infusion: (Simponi Aria): ADULTS, Induration of 5 mm or greater with tuber-
ELDERLY: 2 mg/kg at wk 0, 4 then q8wks culin skin test should be considered a pos-
thereafter. itive result when assessing for latent TB.
Antifungal therapy should be considered
Ulcerative Colitis for those who reside or travel to regions
SQ: (Simponi): ADULTS, ELDERLY: Ini- where mycoses are endemic. Question his-
tially, 200 mg, then 100 mg 2 wks later, tory of anemia, HF, CNS disorders, hepatic
and then 100 mg q4wks thereafter. impairment, HIV, malignancies. Assess
skin for moles, lesions. Receive full medi-
Dosage in Renal/Hepatic Impairment cation history including herbal products.
No dose adjustment.
INTERVENTION/EVALUATION
SIDE EFFECTS Monitor CBC, LFT every 4–8 wks, then pe-
Frequent (13%): Laryngitis, nasophar- riodically. Screen pts for TB (night sweats,
yngitis, pharyngitis, rhinitis, upper re- hemoptysis, weight loss, fever) regardless
spiratory tract infection. Occasional of baseline tuberculin skin test result.
(3%–2%): Bronchitis, hypertension, rash, Monitor hepatitis B virus carriers during
pyrexia. Rare (less than 1%): Dizziness, treatment and several mos after treatment.
paresthesia, constipation. If any viral reactivation occurs, interrupt
treatment and consider antiviral therapy.
ADVERSE EFFECTS/TOXIC Discontinue treatment if acute infection,
REACTIONS opportunistic infection, or sepsis occurs,
Neutropenia, lymphopenia may increase and initiate appropriate antimicrobial
risk of infection. New-onset psoriasis, therapy. Routinely assess skin for new le-
exacerbation of preexisting psoriasis sions. Peripheral edema, difficulty breath-
have been reported. Serious infections ing, coarse crackles on lung auscultation,
including sepsis, pneumonia, cellulitis, elevated BNP may indicate worsening HF.
TB, invasive fungal infections reported. Monitor for hypersensitivity reactions.
May increase risk of lymphoma, mela-
Canadian trade name Non-Crushable Drug High Alert drug
550 goserelin
PATIENT/FAMILY TEACHING PRECAUTIONS
• Treatment may depress your immune Contraindications: Hypersensitivity to
system and reduce your ability to fight goserelin, GnRH, GnRH agonist ana-
infection. Report symptoms of infection logues. Pregnancy (except when used for
such as body aches, chills, cough, fa- palliative treatment of advanced breast
tigue, fever. Avoid those with active infec- cancer). Cautions: Women of childbear-
tion. • Do not receive live vac- ing potential until pregnancy has been
cines. • Report history of HIV, fungal excluded. Pts at risk for decreased bone
infections, HF, hepatitis B, multiple scle- density; diabetes.
rosis, TB, or close relatives who have
active TB. Report travel plans to possible ACTION
G endemic areas. Blood levels, TB screen- Initially, stimulates release of luteinizing
ing will be routinely monitored. • Hives, hormone (LH) and follicle-stimulating
swelling of face, difficulty breathing may hormone (FSH) from anterior pitu-
indicate allergic reaction. • Do not itary. Chronic administration causes a
breastfeed. • Abdominal pain, yellow- sustained suppression of pituitary go-
ing of skin or eyes, dark-amber urine, nadotropins. Therapeutic Effect: In
clay-colored stools, fatigue, loss of ap- females, reduces ovarian, uterine, mam-
petite may indicate liver prob- mary gland size; regresses hormone-
lems. • Decreased platelet count may responsive tumors. In males, decreases
increase risk of bleeding. • Swelling of testosterone level, reduces growth of
hands or feet, difficulty breathing may abnormal prostate tissue.
indicate HF.
PHARMACOKINETICS
Protein binding: 27%. Metabolized in
liver. Excreted in urine. Half-life: 4.2
goserelin hrs (male); 2.3 hrs (female).
goe-se-rel-in LIFESPAN CONSIDERATIONS
(Zoladex, Zoladex LA ) Pregnancy/Lactation: Crosses pla-
centa; unknown if distributed in breast
uCLASSIFICATION
milk. Children: Safety and efficacy not
PHARMACOTHERAPEUTIC: Gonado- established. Elderly: No age-related
tropin-releasing hormone analogue. precautions noted.
CLINICAL: Antineoplastic.
INTERACTIONS
DRUG: Medications prolonging
USES the QT interval (e.g., amiodarone,
Treatment of locally confined prostate azithromycin, ceritinib, haloperi-
cancer. Palliative treatment of advanced dol, moxifloxacin) may increase risk
carcinoma of prostate as alternative when of QT interval prolongation, cardiac
orchiectomy, estrogen therapy is either arrhythmias. HERBAL: None signifi-
not indicated or unacceptable. In com- cant. FOOD: None known. LAB VAL-
bination with an antiestrogen before and UES: May increase serum prostatic
during radiation therapy for early stages acid phosphatase, testosterone, cal-
of prostate cancer. Management of endo- cium; Hgb A1c.
metriosis. Treatment of advanced breast
cancer in premenopausal and perimeno- AVAILABILITY (Rx)
pausal women. Endometrial thinning Injection, Implant: (Zoladex): 3.6 mg,
before ablation for dysfunctional uterine 10.8 mg.
bleeding.

underlined – top prescribed drug


goserelin 551

ADMINISTRATION/HANDLING ADVERSE EFFECTS/TOXIC


SQ Implant REACTIONS
• Administer implant by inserting nee- Arrhythmias, HF, hypertension occur rarely.
dle at 30- to 45-degree angle into ante- Ureteral obstruction, spinal cord compres-
rior abdominal wall below the navel sion have been observed (immediate or-
line. Do not attempt to eliminate air chiectomy may be necessary). Hypersensi-
bubbles or aspirate prior to injection. tivity reactions, including anaphylaxis, may
Do not penetrate into muscle or perito- occur. Hyperglycemia, new-onset diabetes
neum. occurred in men taking GnRH antagonists.
Increased risk of MI, sudden cardiac death
INDICATIONS/ROUTES/DOSAGE was reported. Injection site injuries includ-
Prostatic Carcinoma, Advanced ing hematoma, hemorrhage, hemorrhagic G
SQ: ADULTS OLDER THAN 18 YRS, EL- shock may require blood transfusion or
DERLY:3.6 mg every 28 days or 10.8 mg surgical intervention.
q12wks subcutaneously into upper ab-
dominal wall. NURSING CONSIDERATIONS
BASELINE ASSESSMENT
Prostate Carcinoma, Locally Confined
SQ: ADULTS, ELDERLY: (in combination Question history of diabetes, cardiovascu-
with an antiestrogen and radiotherapy, lar disease, recent MI, prior hypersensitiv-
begin 8 wks prior to radiotherapy): ity reaction. Receive full medication his-
3.6 mg once. 28 days after initial dose, tory; screen for QT interval–prolonging
give 10.8 mg or 3.6 mg q28days for 4 medications, anticoagulant medications.
doses. Screen for conditions predisposing to QT
interval prolongation. In males, question
Breast Carcinoma, Endometriosis history of urethral obstruction, urinary re-
SQ: ADULTS: 3.6 mg every 28 days (6 tention, spinal cord compression, spinal
mos for endometriosis). Subcutane- stenosis. Obtain urine pregnancy. If appli-
ously into upper abdominal wall. cable, obtain bone density test.
Endometrial Thinning INTERVENTION/EVALUATION
SQ: ADULTS: 3.6 mg subcutaneously Monitor pt closely for worsening signs/
into upper abdominal wall as a single symptoms of prostatic cancer, esp. dur-
dose or in 2 doses 4 wks apart. ing first mo of therapy.
Endometriosis PATIENT/FAMILY TEACHING
SQ: ADULTS: 3.6 mg every 28 days for • Use nonhormonal methods of contracep-
6 mos. tion during therapy. • Report suspected
pregnancy or if regular menstruation does
Dosage in Renal/Hepatic Impairment not cease. • Breakthrough menstrual
No dose adjustment. bleeding may occur if dose is missed. • Im-
mediately report sudden weakness, paraly-
SIDE EFFECTS sis, numbness, tingling; difficulty urinating,
Frequent (60%–13%): Headache, hot bladder distention. • Do not take newly
flashes, depression, diaphoresis, sexual prescribed medications unless approved by
dysfunction, impotence, lower urinary prescriber who originally started treat-
tract symptoms. Occasional (10%– ment. • Severe bleeding may occur at the
5%): Pain, lethargy, dizziness, insomnia, injection site, esp. in pts who take blood-
anorexia, nausea, rash, upper respira- thinning medication. • Pts with heart dis-
tory tract infection, hirsutism, abdominal ease are at an increased risk of heart attack
pain. Rare: Pruritus. or sudden death.

Canadian trade name Non-Crushable Drug High Alert drug


552 granisetron
Half-life: 10–12 hrs (increased in el-
granisetron derly).
gra-nis-e-tron LIFESPAN CONSIDERATIONS
(Sancuso, Sustol) Pregnancy/Lactation: Unknown if dis-
Do not confuse granisetron tributed in breast milk. Children: Safety
with alosetron, cilansetron, and efficacy not established in pts younger
dolasetron, ondansetron, or than 2 yrs. Elderly: No age-related pre-
palonosetron. cautions noted.
uCLASSIFICATION INTERACTIONS
G PHARMACOTHERAPEUTIC: Selec- DRUG: QT interval–prolonging medica-
tive serotonin receptor antagonist tions (e.g., amiodarone, azithromycin,
(5-HT3). CLINICAL: Antiemetic. ceritinib, haloperidol, moxifloxacin)
may increase risk of QT interval prolonga-
USES tion, cardiac arrhythmias. SSRIs (e.g.,
Prevention of nausea /vomiting associ- escitalopram, PARoxetine, sertraline),
ated with emetogenic cancer therapy SNRIs (e.g., DULoxetine, venlafaxine)
and cancer radiation therapy. OFF-LABEL: may increase risk of serotonin syndrome.
Prevention, treatment of postop nausea, HERBAL: None significant. FOOD: None
vomiting. Breakthrough treatment of che- known. LAB VALUES: May increase serum
motherapy-associated nausea/vomiting. ALT, AST.

PRECAUTIONS AVAILABILITY (Rx)


Contraindications: ­Hypersensitivity to Injection: (Extended-Release [Sustol]): 10
grani­setron. Hypersensitivity to other mg/0.4 mL single-dose syringe. Injec-
5-HT3 receptor antagonists. Cau- tion Solution: 1 mg/mL. Tablets: 1 mg.
tions: Congenital QT prolongation, con- Transdermal Patch: (Sancuso): 52-cm2
comitant administration of medications patch containing 34.3 mg granisetron
that prolong QT interval, electrolyte delivering 3.1 mg/24 hrs.
abnormalities, cumulative high-dose an- ADMINISTRATION/HANDLING
thracycline therapy. Following abdominal
surgery or in chemotherapy-induced IV
nausea, vomiting (may mask progres-
Reconstitution • May be given undi-
sive ileus or gastric distention), hepatic
luted or dilute with 20–50 mL 0.9% NaCl or
disease.
D5W. Do not mix with other medications.
ACTION Rate of administration • May give
undiluted as IV push over 30 sec. • For
Selectively blocks serotonin stimulation
IV piggyback, infuse over 5–10 min de-
at receptor sites centrally in chemo-
pending on volume of diluent used.
receptor trigger zone, peripherally on
Storage • Appears as a clear, color-
vagal nerve terminals. Therapeutic Ef-
less solution. • Store at room tempera-
fect: Prevents nausea/vomiting.
ture. • After dilution, stable for 3 days
PHARMACOKINETICS at room temperature or 7 days if refriger-
ated. • Inspect for particulates, discol-
Route Onset Peak Duration
oration.
IV 1–3 min N/A 24 hrs
PO
Rapidly, widely distributed to tissues. Pro- • Give 30 min to 1 hr prior to initiating
tein binding: 65%. Metabolized in liver. chemotherapy.
Excreted in urine (48%), feces (38%).
underlined – top prescribed drug
granisetron 553
SQ Prevention of Radiation-Induced Nausea/
Administer in skin of back of upper arm, Vomiting
abdomen (at least 1 inch away from um- PO: ADULTS, ELDERLY: 2 mg once daily,
bilicus). Avoid areas of compromised given 1 hr before radiation therapy.
skin. Administer over 20–30 sec.
Postop Nausea/Vomiting
Transdermal IV: ADULTS, ELDERLY: 0.35–3 mg (5–20
• Apply to clean, dry intact skin on up- mcg/kg) given at end of surgery.
per outer arm. • Remove immediately
from pouch before application. • Do Dosage in Renal/Hepatic Impairment
not cut patch. No dose adjustment. (Sustol): Moder-
ate impairment: No more frequently
G
IV INCOMPATIBILITIES than 14 days. Severe impairment: Not
Amphotericin B (Fungizone). recommended.

IV COMPATIBILITIES SIDE EFFECTS


Allopurinol (Aloprim), bumetanide (Bu- Frequent (21%–14%): Headache, con-
mex), calcium gluconate, CARBOplatin stipation, asthenia. Occasional (8%–
6%): Diarrhea, abdominal pain. Rare
(Paraplatin), CISplatin (Platinol), cy-
(less than 2%): Altered taste, fever.
clophosphamide (Cytoxan), cytarabine
(Ara-C), dacarbazine (DTIC-Dome), ADVERSE EFFECTS/TOXIC
dexamethasone (Decadron), dexmedeto- REACTIONS
midine (Precedex), diphenhydrAMINE
(Benadryl), DOCEtaxel (Taxotere), Hypersensitivity reaction, hypertension,
DOXOrubicin (Adriamycin), etoposide hypotension, arrhythmias (sinus bra-
(VePesid), gemcitabine (Gemzar), mag- dycardia, atrial fibrillation, AV block,
nesium, mitoXANTRONE (Novantrone), ventricular ectopy), ECG abnormalities
PACLitaxel (Taxol), potassium. occur rarely. Increased risk of serotonin
syndrome reported in pts taking con-
INDICATIONS/ROUTES/DOSAGE comitant serotonergic drugs (e.g., SSRIs,
SNRIs). May prolong QTc interval.
Prevention of Chemotherapy-Induced
Nausea/Vomiting NURSING CONSIDERATIONS
PO: ADULTS, ELDERLY: 2 mg up to 1 hr
before chemotherapy or 1 mg up to 1 hr BASELINE ASSESSMENT
before chemotherapy, with a second dose Assess hydration status. Ensure that
12 hrs later. granisetron is given within 30 min of start-
IV: ADULTS, ELDERLY, CHILDREN 2 YRS AND ing chemotherapy. Receive full medication
OLDER: 10 mcg/kg/dose (Maximum: 1 history and screen for interactions. Screen
mg/dose) within 30 min of chemother- for QT interval–prolonging conditions.
apy. Maximum: 1 mg.
INTERVENTION/EVALUATION
SQ: ADULTS, ELDERLY: In combination
with dexamethasone: 10 mg at least Monitor for therapeutic effect. Assess for
30 min before chemotherapy. Do not re- headache. Monitor for dehydration due
peat more frequently than 7 days. to recurrent vomiting. Monitor daily pat-
Transdermal: ADULTS, ELDERLY: Apply tern of bowel activity, stool consistency.
24–48 hrs prior to chemotherapy. Re- PATIENT/FAMILY TEACHING
move minimum 24 hrs after completion
of chemotherapy. May be worn up to • Granisetron is effective shortly follow-
7 days, depending on chemotherapy ing administration; prevents nausea/vom-
duration. iting. • Transitory taste disorder may
occur.

Canadian trade name Non-Crushable Drug High Alert drug


554 guselkumab
ent in breast milk and is known to cross
guselkumab placenta. Children: Safety and efficacy
not established. Elderly: No age-related
gue-sel-koo-mab precautions noted.
(Tremfya)
Do not confuse guselkumab INTERACTIONS
with golimumab, infliximab, DRUG: May enhance adverse/toxic effects,
secukinumab. diminish therapeutic effects of natali-
zumab, vaccines (live). May decrease
uCLASSIFICATION
therapeutic effect of BCG (intravesical).
PHARMACOTHERAPEUTIC: Interleu- HERBAL: Echinacea may decrease effect.
G kin-23 inhibitor. Monoclonal anti- FOOD: None known. LAB VALUES: May
body. CLINICAL: Antipsoriasis agent. increase serum ALT, AST.
AVAILABILITY (Rx)
USES
Injection, Solution: 100 mg/mL in pen-
Treatment of moderate to severe plaque injector, prefilled syringe.
psoriasis in adult pts who are candidates
for systemic therapy or phototherapy. ADMINISTRATION/HANDLING
SQ
PRECAUTIONS
Preparation • Remove prefilled sy-
Contraindications: Hypersensitivity to ringe from refrigerator and allow to
guselkumab. Cautions: Hepatic impair- warm to room temperature (approx. 30
ment, active infection until resolved, his- mins) with needle cap intact. • Visually
tory of chronic or recurrent infections, inspect for particulate matter or discol-
conditions predisposing to infection oration. Solution should appear clear,
(e.g., diabetes, immunocompromised colorless to slightly yellow in color; may
pts, open wounds), prior tuberculosis contain small translucent particles. Do
exposure (do not give to pts with active not use if solution is cloudy, discolored,
TB infection). Concomitant use of live or if large particles are observed. • Dis-
vaccines not recommended. card unused portions.
Administration • Insert needle sub-
ACTION
cutaneously into back of upper arms,
Selectively binds to interleukin-23 recep- front of thighs, or into lower abdomen
tor reducing levels of IL-17A, IL-17F, IL-22. (except for 2 inches around navel), and
IL-23 is a cytokine that is involved in in- inject solution. • Do not inject into ar-
flammatory and immune responses. Ther- eas of the skin where it is tender, bruised,
apeutic Effect: Inhibits release of pro- red, hard, thick, scaly, or affected by
inflammatory cytokines and chemokines. psoriasis. • Rotate injection sites.
Storage • Refrigerate prefilled sy-
PHARMACOKINETICS
ringes in original carton until time of
Widely distributed. Degraded into small use. • Do not freeze. • Do not
peptides and amino acids via catabolic shake. • Protect from light.
pathways. Peak plasma concentration:
5.5 days. Elimination not specified. Half- INDICATIONS/ROUTES/DOSAGE
life: 15–18 days. Plaque Psoriasis
SQ: ADULTS, ELDERLY: 100 mg at wk 0,
LIFESPAN CONSIDERATIONS
wk 4, and then q8wks thereafter.
Pregnancy/Lactation: Unknown if
distributed in breast milk; however, hu- Dosage in Renal/Hepatic Impairment
man immunoglobulin G (IgG) is pres- Not specified; use caution.

underlined – top prescribed drug


guselkumab 555

SIDE EFFECTS dermatologic exam; record characteris-


Occasional (5%–2%): Headache, tension tics of psoriatic lesions. Assess pt’s will-
headache, arthralgia, diarrhea. ingness to self-inject medication.
INTERVENTION/EVALUATION
ADVERSE EFFECTS/TOXIC
REACTIONS Monitor LFT periodically. Monitor for
symptoms of tuberculosis, including
May increase risk of tuberculosis infec-
those who tested negative for latent tu-
tion. Other infections including upper re-
berculosis infection prior to initiating
spiratory tract infection, nasopharyngitis,
therapy. Interrupt or discontinue treat-
pharyngitis, viral upper respiratory tract
ment if serious infection, opportunistic
infection (14% of pts), gastroenteritis,
infection, or sepsis occurs, and initiate G
viral gastroenteritis (1% of pts), tinea in-
appropriate antimicrobial therapy. Assess
fections (1% of pts), herpes simplex virus
skin for improvement of lesions.
(1% of pts) may occur. Mild to moder-
ate elevated serum ALT, AST reported in PATIENT/FAMILY TEACHING
3% of pts. Immunogenicity (auto-gusel- • A health care provider will show you
kumab antibodies) occurred in 6% of pts. how to properly prepare and inject your
medication. You must demonstrate cor-
NURSING CONSIDERATIONS rect preparation and injection techniques
BASELINE ASSESSMENT before using medication at home.
Obtain LFT in pts with hepatic impair- • Treatment may depress your immune
ment. Question history of hepatic im- system response and reduce your ability
pairment, herpes zoster infection, to fight infection. Report symptoms of
parasitic infection. Screen for active infection such as body aches, chills,
infection. Pts should be evaluated for cough, fatigue, fever. Avoid those with
active ­tuberculosis and tested for latent active infection. • Do not receive live
infection prior to initiating treatment and vaccines. • Expect frequent tuberculo-
periodically during therapy. Induration sis screening. Report travel plans to pos-
of 5 mm or greater with tuberculin skin sible endemic areas. • Report liver
testing should be considered a positive problems such as abdominal pain, bruis-
test result when assessing if treatment for ing, clay-colored stool, yellowing of the
latent tuberculosis is necessary. Conduct skin or eyes.

Canadian trade name Non-Crushable Drug High Alert drug


556 haloperidol
ACTION
haloperidol Nonselectively blocks postsynaptic DOP­
amine receptors in brain. Therapeutic
hal-o-per-i-dol Effect: Produces tranquilizing effect.
(Haldol, Haldol Decanoate, Novo- Strong extrapyramidal, antiemetic effects;
Peridol ) weak anticholinergic, sedative effects.
j BLACK BOX ALERT j Increased
risk of mortality in elderly pts with PHARMACOKINETICS
dementia-related psychosis with
use of injections. Readily absorbed from GI tract. Protein
Do not confuse Haldol with binding: 92%. Metabolized in liver. Ex-
Halcion or Stadol. creted in urine. Not removed by hemodi-
alysis. Half-life: 20 hrs.
uCLASSIFICATION
H PHARMACOTHERAPEUTIC: First-
LIFESPAN CONSIDERATIONS
generation (typical) antipsychotic. Pregnancy/Lactation: Crosses pla-
CLINICAL: Antipsychotic, antiemetic, centa. Distributed in breast milk. Chil-
antidyskinetic. dren: More susceptible to dystonias; not
recommended in pts younger than 3 yrs.
Elderly: More susceptible to orthostatic
hypotension, anticholinergic effects, se-
USES dation; increased risk for extrapyramidal
Treatment of schizophrenia, Tourette’s effects. Decreased dosage recommended.
disorder (controls tics and vocal utter-
ances), severe behavioral problems in INTERACTIONS
children with combative explosive hy- DRUG: Alcohol, other CNS depressants
perexcitability without immediate prov- (e.g., diphenhydrAMINE, gabapentin,
ocation. Management of psychotic dis- LORazepam, morphine) may increase
order, short-term treatment of CNS depression. CYP3A4 inducers (e.g.,
hyperactive children. OFF-LABEL: Treat- carBAMazepine, phenytoin, rifAMPin)
ment of nonschizophrenic psychosis, may decrease concentration. Medications
alcohol dependence, psychosis/agita- prolonging QT interval (e.g., amioda-
tion related to Alzheimer’s dementia, rone, ciprofloxacin, ondansetron) may
emergency sedation of severely agitated/ increase risk of QT prolongation. Aclidin-
psychotic pts. ium, ipratropium, tiotropium, ume-
clidinium may increase anticholinergic
PRECAUTIONS effect. Metoclopramide may increase
Contraindications: Hypersensitivity to adverse effects. HERBAL: ­Herbals with
haloperidol, CNS depression, coma, Par- sedative properties (e.g., chamomile,
kinson’s disease. Cautions: Renal/he- kava, kava, v­alerian) may increase CNS
patic impairment, cardiovascular dis- depression. St. John’s wort may decrease
ease, history of seizures, prolonged QT concentration/effect. FOOD: None known.
syndrome, medications that prolong QT LAB VALUES: None significant. Therapeu-
interval, hypothyroidism, thyrotoxicosis, tic serum level: 0.2–1 mcg/mL; toxic se-
electrolyte imbalance (e.g., hypokalemia, rum level: Greater than 1 mcg/mL.
hypomagnesemia), EEG abnormalities,
narrow–angle glaucoma, elderly, pts at AVAILABILITY (Rx)
risk for pneumonia, decreased GI motil- Injection, Oil: (Decanoate): 50 mg/mL,
ity, urinary retention, BPH, visual distur- 100 mg/mL. Injection, Solution: (Lac-
bances, myelosuppression. Pts at risk for tate): 5 mg/mL. Oral Concentrate: 2 mg/
orthostatic hypotension (e.g., cerebro- mL. Tablets: 0.5 mg, 1 mg, 2 mg, 5 mg,
vascular disease). 10 mg, 20 mg.
underlined – top prescribed drug
haloperidol 557

ADMINISTRATION/HANDLING morphine, nitroglycerin, norepinephrine


(Levophed), propofol (Diprivan).
IV

b ALERT c Only haloperidol lactate is INDICATIONS/ROUTES/DOSAGE


given IV. Usual Dosage
Note: For IV administration, ECG moni- IM: (Lactate): ADULTS, ELDERLY: 2–5 mg
toring for QT prolongation/arrhythmias q4–8h as needed. CHILDREN 6–12 YRS: 1–3
is recommended. mg/dose q4–8h as needed. Maxi-
Reconstitution • May give undi- mum: 0.15 mg/kg/day. Change to PO as
luted. • May add to 50–100 mL of D5W. soon as possible. (Decanoate): ADULTS,
Rate of administration • Give IV ELDERLY: Initially, 10–20 times stabilized
push at rate of 5 mg/min. • Infuse IV oral dose. Maximum Initial Dose: 100
piggyback over 30 min. • For IV infu- mg (doses greater the 100 mg should be
sion, up to 25 mg/hr has been used (ti- given as 2 separate injections 3–7 days H
trated to pt response). apart). Maintenance: 10–15 times daily
Storage • Discard if precipitate forms, oral dose or 50–200 mg q4wks.
discoloration occurs. • Store at room PO: ADULTS: 0.5–5 mg 2–3 times/
temperature; do not freeze. • Protect day. Usual dose: 5–20 mg/day. Maxi-
from light. mum: 100 mg/day. ELDERLY: 0.2–2 mg/
day. Usual dose: 5–20 mg/day. Maxi-
IM mum: 100 mg/day. CHILDREN WEIGHING
Parenteral administration • Pt MORE THAN 40 KG, ADOLESCENTS: 0.5–15 mg/
should remain recumbent for 30–60 day in 2–3 divided doses. May increase at no
min to minimize hypotensive ef- less than 5–7 days. Maximum: 15 mg/day.
fect. • Prepare Decanoate IM injection CHILDREN 3–12 YRS, 15–40 KG: Initially, 0.5 mg/
using 21-gauge needle. • Do not ex- day in 2–3 divided doses. May increase by 0.5
ceed maximum volume of 3 mL per IM mg q5–7days. Range: 0.05–0.15 mg/kg/day in
injection site. • Inject slow, deep IM 2–3 divided doses. Maximum: 15 mg/day.
into upper outer quadrant of gluteus
maximus. Tourette’s Disorder
Initially,
PO: CHILDREN 3–12 YRS, 15–40 KG:
PO 0.25–0.5 mg/day in 2–3 divided doses.
• Give without regard to food. • May increase by 0.5 mg/day e­very 5–7
Scored tablets may be crushed. • Dilute days to usual dose of 1–4 mg/day. CHIL-
oral concentrate with water or juice. DREN WEIGHING MORE THAN 40 KG, ADOLES-
• Avoid skin contact with oral concen- CENTS: Initially, 0.25–0.5 mg/day in 2–3
trate; may cause contact dermatitis. divided doses. May increase as needed ev-
ery 5–7 days to usual dose of 1–4 mg/day.
IV INCOMPATIBILITIES
Allopurinol (Aloprim), amphotericin B Dosage in Renal/Hepatic Impairment
complex (Abelcet, AmBisome, Ampho- No dose adjustment.
tec), cefepime (Maxipime), fluconazole
(Diflucan), foscarnet (Foscavir), hepa- SIDE EFFECTS
rin, nitroprusside (Nipride), piperacil- Frequent: Blurred vision, constipation,
lin/tazobactam (Zosyn). orthostatic hypotension, dry mouth,
swelling or soreness of female breasts,
IV COMPATIBILITIES peripheral edema. Occasional: Allergic
DOBUTamine (Dobutrex), DOPamine reaction, difficulty urinating, decreased
(Intropin), fentaNYL (Sublimaze), HY- thirst, dizziness, diminished sexual func-
DROmorphone (Dilaudid), lidocaine, LO- tion, drowsiness, nausea, vomiting, pho-
Razepam (Ativan), midazolam (Versed), tosensitivity, lethargy.

Canadian trade name Non-Crushable Drug High Alert drug


558 heparin

ADVERSE EFFECTS/TOXIC r­equire alertness, motor skills until re-


REACTIONS sponse to drug is established. • Avoid
Extrapyramidal symptoms (EPS) appear to ­alcohol. • Report muscle stiffness, lip
be dose related and typically occur in first puckering, tongue protrusion, restlessness.
few days of therapy. Marked drowsiness/ • Avoid overheating, dehydration, exposure
lethargy, excessive salivation, fixed stare to sunlight (increased risk of heatstroke).
may be mild to severe in intensity. Less fre-
quently noted are severe akathisia (motor
restlessness), acute dystonias: torticollis
(neck muscle spasm), opisthotonos (ri- heparin
gidity of back muscles), oculogyric crisis
(rolling back of eyes). Tardive dyskinesia hep-a-rin
(tongue protrusion, puffing of cheeks, (Hepalean Leo )
H chewing/puckering of the mouth) may oc- Do not confuse heparin with
cur during long-term therapy or after drug Hespan.
discontinuance and may be irreversible. El- uCLASSIFICATION
derly female pts have greater risk of devel-
oping this reaction. May increase risk of QT PHARMACOTHERAPEUTIC: Blood
interval prolongation, cardiac arrhythmias. modifier. CLINICAL: Anticoagulant.

NURSING CONSIDERATIONS
USES
BASELINE ASSESSMENT Prophylaxis and treatment of thrombo-
Assess behavior, appearance, emotional embolic disorders and thromboembolic
status, response to environment, speech complications associated with atrial fi-
pattern, thought content. Assess mental brillation; anticoagulant for extracorpo-
status. Screen for co-morbidities as listed real and dialysis procedures; maintain
in Precautions (esp. seizure disorder, patency of IV devices. Prevents clotting in
long QT syndrome). arterial and cardiac surgery. OFF-LABEL:
INTERVENTION/EVALUATION
STEMI, non-STEMI, unstable angina,
anticoagulant used during percutaneous
Monitor B/P, heart rate/rhythm. Monitor coronary intervention.
ECG, QT interval. Supervise suicidal-risk
pts closely during early therapy (as de- PRECAUTIONS
pression lessens, energy level improves, Contraindications: Hypersensitivity to hep­
increasing suicide potential). Monitor arin. Severe thrombocytopenia, uncon-
for rigidity, tremor, mask-like facial ex- trolled active bleeding (unless secondary
pression, fine tongue movement. Assess to disseminated intravascular coagula-
for therapeutic response (interest in tion [DIC]), history of heparin-induced
surroundings, improvement in self-care, thrombocytopenia (HIT), heparin-induced
increased ability to concentrate, relaxed thrombocytopenia with thrombosis (HITT),
facial expression). Therapeutic serum or pts who test positive for HIT antibody.
level: 0.2–1 mcg/mL; toxic serum Cautions: Allergy to pork. Pts at risk for
level: greater than 1 mcg/mL. bleeding (e.g., congenital/acquired bleed-
PATIENT/FAMILY TEACHING ing disorders, active GI ulcerative disease,
• Full therapeutic effect may take up to 6 hemophilia, concomitant platelet inhibi-
wks. • Do not abruptly withdraw from tors, severe hypertension, menses, recent
long-term drug therapy. • Sugarless gum, lumbar puncture or spinal anesthesia; re-
sips of water may relieve dry mouth. cent major surgery, trauma). Use of preser-
• Drowsiness generally subsides during vative-free heparin recommended in neo-
con­tinued therapy. • Avoid tasks that nates, infants, pregnant or nursing mothers.

underlined – top prescribed drug


heparin 559

ACTION Solution for Infusion:25,000 units/250 mL


Potentiates action of antithrombin III. infusion, 25,000 units/500 mL infusion.
Interferes with blood coagulation by ADMINISTRATION/HANDLING
blocking conversion of prothrombin
to thrombin and fibrinogen to fibrin. b ALERT c Do not give by IM injection
Therapeutic Effect: Prevents further (pain, hematoma, ulceration, erythema).
extension of existing thrombi or new clot IV
formation. No effect on existing clots.
b ALERT c Used in full-dose therapy.
PHARMACOKINETICS Intermittent IV dosage produces higher
Well absorbed following SQ administra- incidence of bleeding abnormalities.
tion. Protein binding: Very high. Metabo- Continuous IV route preferred.
lized in liver. Removed from circulation Reconstitution • Premix solution re-
via uptake by reticuloendothelial system. quires no reconstitution. H
Primarily excreted in urine. Not removed Rate of administration • Infuse and
by hemodialysis. Half-life: 1–6 hrs. titrate per protocol using infusion pump.
Storage • Store at room temperature.
LIFESPAN CONSIDERATIONS
SQ
Pregnancy/Lactation: Use with cau-
b ALERT c Used in low-dose therapy.
tion, particularly during last trimester,
• After withdrawal of heparin from vial,
immediate postpartum period (increased
change needle before injection (prevents
risk of maternal hemorrhage). Does not
leakage along needle track). • Inject
cross placenta. Not distributed in breast
above iliac crest or in abdominal fat layer.
milk. Children: No age-related precau-
Do not inject within 2 inches of umbilicus
tions noted. Benzyl alcohol preservative
or any scar tissue. • Withdraw needle
may cause gasping syndrome in infants.
rapidly, apply prolonged pressure at injec-
Elderly: More susceptible to hemor-
tion site. Do not massage or apply heat/cold
rhage. Age-related renal impairment may
to injection site. • Rotate injection sites.
increase risk of bleeding.
IV INCOMPATIBILITIES
INTERACTIONS
Amiodarone (Cordarone), amphotericin B
DRUG: Anticoagulants (e.g., apixa- complex (Abelcet, AmBisome, Amphotec),
ban, dabigatran, rivaroxaban, ciprofloxacin (Cipro), dacarbazine (DTIC),
warfarin) may increase anticoagu- diazePAM (Valium), DOBUTamine (Dobu-
lant effect; risk of bleeding. plate- trex), DOXOrubicin (Adriamycin), filgrastim
let aggregation inhibitors (e.g., (Neupogen), gentamicin (Garamycin), halo-
aspirin), thrombolytics (e.g., peridol (Haldol), IDArubicin (Idamycin), la-
tissue plasminogen activator betalol (Trandate), niCARdipine (Cardene),
[TPA]) may increase risk of bleeding. phenytoin (Dilantin), quiNIDine, tobramycin
HERBAL: Herbals with anticoagu- (Nebcin), vancomycin (Vancocin).
lant/antiplatelet properties (e.g.,
garlic, ginger, ginkgo biloba) may IV COMPATIBILITIES
increase risk of bleeding. FOOD: None Ampicillin/sulbactam (Unasyn), aztreonam
known. LAB VALUES: May increase (Azactam), calcium gluconate, ceFAZolin
free fatty acids, serum ALT, AST; aPTT. (Ancef), cefTAZidime (Fortaz), cefTRI-
May decrease serum cholesterol. AXone (Rocephin), dexmedetomidine
(Precedex), digoxin (Lanoxin), dilTIA-
AVAILABILITY (Rx) Zem (Cardizem), DOPamine (Intropin),
10 units/mL, 100 units/
Injection Solution: enalapril (Vasotec), famotidine (Pepcid),
mL, 1,000 units/mL, 5,000 units/mL, fentaNYL (Sublimaze), furosemide (Lasix),
10,000 units/mL, 20,000 units/mL. Premix ­HYDROmorphone (Dilaudid), insulin,
Canadian trade name Non-Crushable Drug High Alert drug
560 heparin
lidocaine, LORazepam (Ativan), magne- ADVERSE EFFECTS/TOXIC
sium sulfate, methylPREDNISolone (Solu- REACTIONS
Medrol), midazolam (Versed), milrinone Bleeding complications ranging from
(Primacor), morphine, nitroglycerin, local ecchymoses to major hemorrhage
norepinephrine (Levophed), oxytocin (cutaneous/GI/genitourinary/intracra-
(Pitocin), piperacillin/tazobactam (Zo- nial/nasal/oral/pharyngeal/urethral/
syn), procainamide (Pronestyl), propo- vaginal bleeding) occur more frequently
fol (Diprivan). in high-dose therapy, intermittent IV in-
INDICATIONS/ROUTES/DOSAGE fusion, women 60 yrs and older. HIT
can cause life-threatening thromboem-
Line Flushing
bolism such as CVA, MI, DVT, pulmo-
IV: ADULTS, ELDERLY, CHILDREN: 100
nary embolism, renal artery thrombo-
units as needed. INFANTS WEIGHING LESS sis, mesenteric thrombosis. Antidote:
H THAN 10 KG: 10 units as needed.
Protamine sulfate 1–1.5 mg IV for every
Acute Coronary Syndrome 100 units heparin SQ within 30 min of
60 units/
IV infusion: ADULTS, ELDERLY: overdose, 0.5–0.75 mg for every 100
kg bolus (Maximum: 4,000 units), then units heparin SQ if within 30–60 min of
12 units/kg/hr (Maximum: 1,000 units/ overdose, 0.25–0.375 mg for every 100
hr as continuous infusion). units heparin SQ if 2 hrs have elapsed
since overdose, 25–50 mg if heparin
Cardiothoracic Surgery was given by IV infusion.
IV: ADULTS, ELDERLY: Initially, 300–400
units/kg before arterial or venous can- NURSING CONSIDERATIONS
nulation. Titrate to ACT. Bypass initiated BASELINE ASSESSMENT
once ACT is at least 400 seconds.
Obtain CBC, PT/INR, aPTT. Cross-check
Treatment of DVT/PE dose with co-worker. Assess for bleeding
IV infusion: ADULTS, ELDERLY: 80 units/ risk. Question history of recent trauma,
kg bolus (Maximum: 5,000 units), then head injuries, GI/GU bleeding. Ensure
18 units/kg/hr adjusted according to aPTT. that pt has not received spinal anesthesia,
spinal procedures.
Usual Pediatric/Neonatal Dose
IV infusion: 75 units/kg bolus over 10 min, INTERVENTION/EVALUATION
then initial maintenance dose of 28 units/ Monitor CBC, PT/INR daily. Obtain aPTT
kg/hr. Adjust dose according to aPTT per 6 hrs after initiation or any change in
protocol. dosage (or per clinical standards) until
maintenance dose is established, then
Thromboembolic Prophylaxis
check aPTT q24hrs (or per clinical
SQ: ADULTS, ELDERLY: 5,000 units q8– standards). In long-term therapy, moni-
12h. tor 1–2 times/mo. Diligently assess for
Dosage in Renal/Hepatic Impairment bleeding. If platelet count decreases
No dose adjustment. more than 50% from baseline, obtain
stat HIT antibody test. If HIT antibody
SIDE EFFECTS positive, discontinue heparin and con-
Occasional: Pruritus, burning (particu- sider treatment with direct thrombin
larly on soles of feet) caused by vaso- inhibitor (e.g., argatroban); avoid all
spastic reaction. Rare: Pain, cyanosis of heparin products and place heparin al-
extremity 6–10 days after initial therapy lergy on chart. Monitor urine and stool
lasting 4–6 hrs, hypersensitivity reaction for occult blood. Assess for decrease in
(chills, fever, pruritus, urticaria, asthma, B/P, increase in pulse rate, complaint of
rhinitis, lacrimation, headache). abdominal/back pain, severe headache

underlined – top prescribed drug


hydrALAZINE 561
(may be evidence of hemorrhage). Ques- secondary to eclampsia, preeclampsia.
tion for increase in amount of discharge Treatment of HF with reduced ejection
during menses. Assess peripheral pulses; fraction, postoperative hypertension.
skin for ecchymosis, petechiae. Check
for excessive bleeding from minor cuts, PRECAUTIONS
scratches. Assess gums for erythema, Contraindications: Hypersensitivity to
gingival bleeding. Assess urine output for hydrALAZINE. Coronary artery disease,
hematuria. Avoid IM injections due to po- mitral valvular rheumatic heart disease.
tential for hematomas. When converting Cautions: Advanced renal impairment,
to warfarin (Coumadin) therapy, monitor cerebrovascular accident, suspected
PT/INR results (will be 10%–20% higher coronary artery disease. Pts with mitral
while heparin is given concurrently). valvular disease, positive ANA titer, pul-
monary hypertension.
PATIENT/FAMILY TEACHING H
• Use electric razor, soft toothbrush to ACTION
prevent bleeding. • Report red or dark Direct vasodilating effects on arterioles.
urine, black or red stool, coffee-ground Therapeutic Effect: Decreases B/P,
vomitus, blood-tinged mucus from systemic vascular resistance.
cough, signs of stroke, nosebleeds, or
increase in menstruation. • Do not use PHARMACOKINETICS
any OTC medication without physician Route Onset Peak Duration
approval (may interfere with platelet ag- PO 20–30 min N/A Up to 8 hrs
gregation). • Wear or carry identifica- IV 5–20 min N/A 1–4 hrs
tion that notes anticoagulant ther-
apy. • Inform dentist, other physicians Well absorbed from GI tract. Widely
of heparin therapy. • Limit alcohol. distributed. Protein binding: 85%–90%.
Metabolized in liver. Primarily excreted
in urine. Not removed by hemodialysis.
Half-life: 3–7 hrs (increased in renal
hydrALAZINE impairment).

hye-dral-a-zeen LIFESPAN CONSIDERATIONS


(Apresoline ) Pregnancy/Lactation: Drug crosses
Do not confuse hydrALAZINE placenta. Unknown if distributed in breast
with hydrOXYzine. milk. Thrombocytopenia, leukopenia,
petechial bleeding, hematomas have oc-
FIXED-COMBINATION(S) curred in newborns (resolved within
Apresazide: hydrALAZINE/hydro- 1–3 wks). Children: No age-­related
CHLOROthiazide (a diuretic): 25 precautions noted. Elderly: More sen-
mg/25 mg, 50 mg/50 mg, 100 mg/50 sitive to hypotensive effects. Age-related
mg. BiDil: hydrALAZINE/isosorbide (a renal impairment may require dosage
nitrate): 37.5 mg/20 mg. ­adjustment.
uCLASSIFICATION INTERACTIONS
PHARMACOTHERAPEUTIC: Vasodila- DRUG: Diuretics (e.g., furosemide,
tor. CLINICAL: Antihypertensive. HCTZ), other antihypertensives
(e.g., amLODIPine, cloNIDine, lisin-
opril, valsartan) may increase hypoten-
USES sive effect. HERBAL: Herbals with hy-
Management of moderate to severe hy- pertensive properties (e.g., licorice,
pertension. OFF-LABEL: Hypertension yohimbe) or hypotensive properties

Canadian trade name Non-Crushable Drug High Alert drug


562 hydrALAZINE
(e.g., garlic, ginger, ginkgo biloba) Dosage in Renal Impairment
may alter effects. FOOD: Any foods may Dosage interval is based on creatinine
increase absorption. LAB VALUES: May clearance.
produce positive direct Coombs’ test. Creatinine Clearance Dosage
10–50 mL/min q8h
AVAILABILITY (Rx) Less than 10 mL/min q12–24h
Injection Solution: 20 mg/mL. Tab-
lets: 10 mg, 25 mg, 50 mg, 100 mg.
Dosage in Hepatic Impairment
ADMINISTRATION/HANDLING No dose adjustment.

IV SIDE EFFECTS
Rate of administration • May give Occasional: Headache, anorexia, nau-
sea, vomiting, diarrhea, palpitations,
H undiluted. • Administer slowly: maxi-
mum rate 5 mg/min (0.2 mg/kg/min for tachycardia, angina pectoris. Rare: Con-
children). stipation, ileus, edema, peripheral neu-
Storage • Store at room temperature.
ritis (paresthesia), dizziness, muscle
cramps, anxiety, hypersensitivity reac-
PO tions (rash, urticaria, pruritus, fever,
• Best given with food at regularly spaced chills, arthralgia), nasal congestion,
meals. • Tablets may be crushed. flushing, conjunctivitis.

IV INCOMPATIBILITIES ADVERSE EFFECTS/TOXIC


Ampicillin (Polycillin), furosemide (Lasix). REACTIONS
High dosage may produce lupus ery-
IV COMPATIBILITIES thematosus–like reaction (fever, facial
DOBUTamine (Dobutrex), heparin, hy- rash, muscle/joint aches, glomerulo-
drocortisone (Solu-Cortef), nitroglyc- nephritis, splenomegaly). Severe or-
erin, potassium chloride. thostatic hypotension, skin flushing,
severe headache, myocardial ischemia,
INDICATIONS/ROUTES/DOSAGE cardiac arrhythmias may develop. Pro-
Hypertension found shock may occur with severe
PO: ADULTS, ELDERLY: Initially, 10 mg overdosage.
4 times/day for first 2–4 days. May in-
crease to 25 mg 4 times/day balance of NURSING CONSIDERATIONS
first wk. May increase by 10–25 mg/ BASELINE ASSESSMENT
dose gradually q2–5 days to 50 mg Obtain B/P, pulse immediately before
4 times/day. Usual range: 100–200 each dose, in addition to regular moni-
mg/day in 2–3 divided doses. CHIL- toring (be alert to fluctuations).
DREN: Initially, 0.75 mg/kg/day in
2–4 divided doses. May increase over INTERVENTION/EVALUATION
3–4 wks. Maximum: 7.5 mg/kg/day Monitor B/P, pulse. Monitor for head-
(7.5 mg/kg/day in infants). Maximum ache, palpitations, tachycardia. Assess for
daily dose: 200 mg/day in divided peripheral edema of hands, feet.
doses.
IV, IM: ADULTS, ELDERLY: Initially, 10–20 PATIENT/FAMILY TEACHING
mg/dose q4–6h. May increase to 40 • To reduce hypotensive effect, go from
mg/dose. CHILDREN: Initially, 0.1–0.2 lying to standing slowly. • Report
mg/kg/dose. Usual range: 0.2–0.6 mg/ muscle/joint aches, fever (lupus-like
­
kg/dose q2–6h as needed. Maximum reaction), flu-like symptoms. • Limit
­
dose: 20 mg. ­alcohol use.

underlined – top prescribed drug


hydroCHLOROthiazide 563
thiazide/triamterene (a potassium-
hydroCHLOROthiazide sparing diuretic): 25 mg/37.5 mg, 25
mg/50 mg, 50 mg/75 mg. Exforge
hye-dro-klor-oh-thy-ah-zide HCT: hydroCHLOROthiazide/amLO-
(Urozide ) DIPine (a calcium channel blocker)/
Do not confuse Microzide with valsartan (an angiotensin II receptor
Maxzide. blocker): 12.5 mg/5 mg/160 mg, 25
mg/5 mg/160 mg, 12.5 mg/10 mg/160
FIXED-COMBINATION(S) mg, 25 mg/10 mg/160 mg, 25 mg/10
Accuretic: hydroCHLOROthiazide/ mg/320 mg. Hyzaar: hydroCHLO-
quinapril (an angiotensin-converting ROthiazide/losartan (an angiotensin
enzyme [ACE] inhibitor): 12.5 mg/10 II receptor antagonist): 12.5 mg/50
mg, 12.5 mg/20 mg, 25 mg/20 mg. mg, 12.5 mg/100 mg, 25 mg/100 mg.
Aldactazide: hydroCHLOROthiazide/ Inderide: hydroCHLOROthiazide/ H
spironolactone (a potassium-sparing propranolol (a beta blocker): 25
diuretic): 25 mg/25 mg, 50 mg/50 mg/40 mg, 25 mg/80 mg, 50 mg/80
mg. Aldoril: hydroCHLOROthiazide/ mg, 50 mg/120 mg, 50 mg/160 mg.
methyldopa (an antihypertensive): Lopressor HCT: hydroCHLOROthia-
15 mg/250 mg, 25 mg/250 mg, 30 zide/metoprolol (a beta blocker): 25
mg/500 mg, 50 mg/500 mg. Am- mg/50 mg, 25 mg/100 mg, 50 mg/100
turnide: hydroCHLOROthiazide/ mg. Lotensin HCT: hydroCHLOROthi-
aliskiren (renin inhibitor)/amLO- azide/benazepril (an ACE inhibitor):
DIPine (calcium channel blocker): 6.25 mg/5 mg, 12.5 mg/10 mg, 12.5
12.5 mg/150 mg/5 mg, 12.5 mg/300 mg/20 mg, 25 mg/20 mg. Micardis
mg/5 mg, 25 mg/300 mg/5 mg, 12.5 HCT: hydroCHLOROthiazide/telmis-
mg/300 mg/10 mg, 25 mg/300 mg/10 artan (an angiotensin II receptor an-
mg. Apresazide: hydroCHLOROthia- tagonist): 12.5 mg/40 mg, 12.5 mg/80
zide/hydrALAZINE (a vasodilator): 25 mg. Moduretic: hydroCHLOROthia-
mg/25 mg, 50 mg/50 mg, 50 mg/100 zide/aMILoride (a potassium-sparing
mg. Atacand HCT: hydroCHLOROthi- diuretic): 50 mg/5 mg. Normozide:
azide/candesartan (an angiotensin II hydroCHLOROthiazide/labetalol (a
receptor antagonist): 12.5 mg/16 mg, beta blocker): 25 mg/100 mg, 25
12.5 mg/32 mg. Avalide: hydroCHLO- mg/300 mg. Prinzide/Zestoretic:
ROthiazide/irbesartan (an angiotensin hydroCHLOROthiazide/lisinopril (an
II receptor antagonist): 12.5 mg/150 ACE inhibitor): 12.5 mg/10 mg, 12.5
mg, 12.5 mg/300 mg, 25 mg/300 mg. mg/20 mg, 25 mg/20 mg. Tekturna
Benicar HCT: hydroCHLOROthiazide/ HCT: hydroCHLOROthiazide/aliski-
olmesartan (an angiotensin II recep- ren (a renin inhibitor): 12.5 mg/150
tor antagonist): 12.5 mg/20 mg, 12.5 mg, 25 mg/300 mg. Teveten HCT:
mg/40 mg, 25 mg/40 mg. Capozide: hydroCHLOROthiazide/eprosartan (an
hydroCHLOROthiazide/captopril (an angiotensin II receptor antagonist):
ACE inhibitor): 15 mg/25 mg, 15 12.5 mg/600 mg, 25 mg/600 mg.
mg/50 mg, 25 mg/25 mg, 25 mg/50 Timolide: hydroCHLOROthiazide/
mg. Diovan HCT: hydroCHLORO- timolol (a beta blocker): 25 mg/10
thiazide/valsartan (an angiotensin mg. Tribenzor: hydroCHLOROthia-
II receptor antagonist): 12.5 mg/80 zide/olmesartan/amLODIPine: 12.5
mg, 12.5 mg/160 mg. Dutoprol: mg/20 mg/5 mg, 12.5 mg/40 mg/5
hydroCHLOROthiazide/metoprolol mg, 25 mg/40 mg/5 mg, 12.5 mg/40
(a beta blocker): 12.5 mg/25 mg, mg/10 mg, 25 mg/40 mg/10 mg. Uni-
12.5 mg/50 mg, 12.5 mg/100 mg. retic: hydroCHLOROthiazide/moexi-
Dyazide/Maxide: hydroCHLORO- pril (an ACE inhibitor): 12.5 mg/7.5

Canadian trade name Non-Crushable Drug High Alert drug


564 hydroCHLOROthiazide
mg, 25 mg/15 mg. Vaseretic: hydro- Children: No age-related precautions
CHLOROthiazide/enalapril (an ACE noted, except jaundiced infants may
inhibitor): 12.5 mg/5 mg, 25 mg/10 be at risk for hyperbilirubinemia. El-
mg. Ziac: hydroCHLOROthiazide/bi- derly: May be more sensitive to hypo-
soprolol (a beta blocker): 6.25 mg/5 tensive, electrolyte effects. Age-related
mg, 6.25 mg/10 mg. renal impairment may require dosage
adjustment.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Sulfona- INTERACTIONS
mide derivative. Thiazide diuretic.
CLINICAL: Antihypertensive.
DRUG: Bile acid sequestrants (e.g.,
cholestyramine, colestipol) Anti-
hypertensives (e.g., amLODIPine,
H USES cloNIDine, lisinopril, valsartan)
may increase hypotensive effect. May
Treatment of mild to moderate hyper- increase risk of digoxin toxicity.
tension, edema in HF, hepatic cirrhosis, May increase risk of lithium toxicity.
renal dysfunction (e.g., nephrotic syn- HERBAL: Herbals with hypertensive
drome). OFF-LABEL: Treatment of cal- properties (e.g., licorice, yohimbe)
cium nephrolithiasis. or hypotensive properties (e.g.,
garlic, ginger, ginkgo biloba) may
PRECAUTIONS alter effects. Licorice may increase hy-
Contraindications: Hypersensitivity to pokalemic effect. FOOD: None known.
hydroCHLOROthiazide. Anuria, history LAB VALUES: May increase serum glu-
of hypersensitivity to sulfonamides or cose, cholesterol, LDL, bilirubin, cal-
thiazide diuretics. Cautions: Severe re- cium, creatinine, uric acid, triglycerides.
nal/hepatic impairment, prediabetes or May decrease urinary calcium, serum
diabetes, elderly or debilitated, history magnesium, potassium, sodium.
of gout, moderate to high serum choles-
terol, hypercalcemia, hypokalemia.
AVAILABILITY (Rx)
ACTION Capsules:12.5 mg. Tablets: 12.5 mg, 25
mg, 50 mg.
Inhibits sodium reabsorption in distal
renal tubules, causing excretion of so-
dium, potassium, hydrogen ions, water. ADMINISTRATION/HANDLING
Therapeutic Effect: Promotes diure- PO
sis; reduces B/P. • May take with or without food. If GI
upset occurs, give with food or milk,
PHARMACOKINETICS preferably with breakfast (may prevent
Route Onset Peak Duration nocturia). • Give last dose no later than
PO (diuretic) 2 hrs 4–6 hrs 6–12 hrs 6 pm unless instructed otherwise.
Variably absorbed from GI tract. Primar-
ily excreted unchanged in urine. Not re- INDICATIONS/ROUTES/DOSAGE
moved by hemodialysis. Half-life: 5.6– Hypertension
14.8 hrs. PO: ADULTS: Initially, 12.5–25 mg
once daily. May increase up to 50 mg
LIFESPAN CONSIDERATIONS once daily. ELDERLY: Initially, 12.5 mg
Pregnancy/Lactation: Crosses pla- once daily. Titrate in 12.5 mg incre-
centa. Small amount distributed in breast ments up to 50 mg/day in 1–2 divided
milk. Breastfeeding not recommended. doses.

underlined – top prescribed drug


HYDROcodone 565
Usual Pediatric Dosage (Edema/HTN) INTERVENTION/EVALUATION
PO: CHILDREN 2–12 YRS: 1–2 mg/kg/ Continue to monitor B/P, vital signs, elec-
day. Maximum: 100 mg/day. CHILDREN trolytes, I&O, daily weight. Note extent of
6 MOS–2 YRS: 1–2 mg/kg/day in 1–2 di- diuresis. Watch for changes from initial
vided doses. Maximum: 37.5 mg/day. assessment (hypokalemia may result
CHILDREN YOUNGER THAN 6 MOS: 1–2 in weakness, tremor, muscle cramps,
mg/kg/day in 2 divided doses. Maxi- nausea, vomiting, altered mental status,
mum: 37.5 mg/day. tachycardia; hyponatremia may result in
confusion, thirst, cold/clammy skin). Be
Dosage in Renal Impairment
esp. alert for potassium depletion in pts
Creatinine clearance less than 30
taking digoxin (cardiac arrhythmias).
mL/min: Generally not effective. Avoid
Potassium supplements are frequently
use with creatinine clearance less than ordered. Check for constipation (may
10 mL/min. occur with exercise diuresis). H
Dosage in Hepatic Impairment PATIENT/FAMILY TEACHING
Use caution. • Expect increased frequency (dimin-
SIDE EFFECTS ishes with continued use), volume of
urination. • To reduce hypotensive ef-
Expected: Increased urinary frequency fect, go from lying to standing
(diminishes with continued use), urine vol- slowly. • Eat foods high in potassium,
ume. Frequent: Potassium depletion. Occa- such as whole grains (cereals), legumes,
sional: Orthostatic hypotension, headache,
meat, bananas, apricots, orange juice,
GI disturbances, photosensitivity. potatoes (white, sweet), raisins. • Pro-
ADVERSE EFFECTS/TOXIC tect skin from sun, ultraviolet light (pho-
REACTIONS tosensitivity may occur).
Vigorous diuresis may lead to profound
water loss/electrolyte depletion, resulting
in hypokalemia, hyponatremia, dehydra-
tion. Acute hypotensive episodes may
HYDROcodone
occur. Hyperglycemia may occur during hye-droe-koe-done
prolonged therapy. Pancreatitis, blood (Hycodan , Hysingla ER, Robi-
dyscrasias, pulmonary edema, allergic done , Zohydro ER)
pneumonitis, dermatologic reactions oc-
cur rarely. Overdose can lead to lethargy, j BLACK BOX ALERT jRisk
of opioid addiction, abuse, and
coma without changes in electrolytes or misuse. Serious, life-threatening,
hydration. or fatal respiratory depression may
occur. Accidental ingestion by chil-
dren can result in fatal overdose.
NURSING CONSIDERATIONS Prolonged use during pregnancy
may result in opioid withdrawal
BASELINE ASSESSMENT syndrome. Concomitant use of
Check vital signs, esp. B/P for hypoten- CYP3A4 inhibitors may increase
sion, before administration. Assess base- concentration/effect. Discon-
tinuation of CYP3A4 inducers may
line electrolytes, esp. for hypokalemia. increase concentration/effect. Con-
Evaluate skin turgor, mucous membranes comitant use of CNS depressants
for hydration status. Evaluate for periph- (e.g., benzodiazepines) may result
eral edema. Assess muscle strength, in profound sedation, respiratory
mental status. Note skin temperature, depression, coma, or death.
moisture. Obtain baseline weight. Moni- Do not confuse Hycodan with
tor I&O. Vicodin.

Canadian trade name Non-Crushable Drug High Alert drug


566 HYDROcodone

FIXED-COMBINATION(S) including paralytic ileus (known or


Hycet: HYDROcodone/acetamino- ­suspected). ­Cautions: Adrenal insuffi-
phen: 7.5 mg/325 mg per 15 mL. ciency, biliary tract disease, pancreatitis,
Hycodan: HYDROcodone/homatro- CNS depression/coma, acute alcoholism,
pine (an anticholinergic): 5 mg/1.5 hypothyroidism; severe renal, hepatic, or
mg. Hycotuss, Vitussin: HYDROco- pulmonary impairment; urinary stricture,
done/guaiFENesin (an expectorant): prostatic hypertrophy, seizures, elderly,
5 mg/100 mg. Norco: HYDROco- debilitated, other CNS depressants, his-
done/acetaminophen: 5 mg/325 tory of substance abuse.
mg, 7.5 mg/325 mg, 10 mg/325 mg. ACTION
Reprexain CIII: HYDROcodone/
ibuprofen (an NSAID): 5 mg/200 Binds with opioid receptors in CNS.
mg. Rezira: HYDROcodone/pseu- Therapeutic Effect: Reduces intensity
H doephedrine (a nasal decongestant): of incoming pain stimuli from sensory
5 mg/60 mg per 5 mL. Tussend: nerve endings, altering pain perception,
HYDROcodone/pseudoephedrine emotional response to pain; suppresses
(a ­sympathomimetic)/guaiFENesin cough reflex.
(an expectorant): 2.5 mg/30 mg/100 PHARMACOKINETICS
mg per 5 mL. Vicodin: HYDROco-
Route Onset Peak Duration
done/acetaminophen: 5 mg/300 mg.
Vicodin ES: HYDROcodone/acet- PO (analgesic) 10–20 30–60 4–6 hrs
min min
aminophen: 7.5 mg/300 mg. Vicodin PO (antitussive) N/A N/A 4–6 hrs
HP: HYDROcodone/acetaminophen:
10 mg/300 mg. Vicoprofen: HY- Well absorbed from GI tract. Metabolized
DROcodone/ibuprofen (an NSAID): in liver. Primarily excreted in urine. Half-
7.5 mg/200 mg. Xodol: HYDRO- life: 3.8 hrs (increased in elderly).
codone/acetaminophen: 5 mg/300
mg, 7.5 mg/300 mg, 10 mg/300 mg. LIFESPAN CONSIDERATIONS
Zutripro: HYDROcodone/chlorphe- Pregnancy/Lactation: Read i l y
niramine (an antihistamine)/pseudo- crosses placenta. Distributed in breast
ephedrine (a nasal decongestant): 5 milk. May prolong labor if administered
mg/4 mg/60 mg. in latent phase of first stage of labor or
before cervical dilation of 4–5 cm has
uCLASSIFICATION
occurred. Respiratory depression may
PHARMACOTHERAPEUTIC: Opioid occur in neonate if mother received opi-
agonist (Schedule III). CLINICAL: Nar- ates during labor. Regular use of opiates
cotic analgesic. during pregnancy may produce with-
drawal symptoms (irritability, excessive
crying, tremors, hyperactive reflexes,
USES fever, vomiting, diarrhea, yawning,
Relief of moderate to moderately se- sneezing, seizures) in the neonate. Chil-
vere pain. Hysingla ER, Zohydro ER: dren: Pts younger than 2 yrs may be
Around-the-clock management of moder- more susceptible to respiratory depres-
ate to severe chronic pain. sion. Elderly: May be more susceptible
to respiratory depression, may cause
PRECAUTIONS paradoxical excitement. Age-related
Contraindications:Hypersensitivity to renal impairment, prostatic hypertro-
HYDROcodone. Significant respiratory phy or obstruction may increase risk
depression, acute or severe bronchial of urinary retention; dosage adjustment
asthma or hypercarbia, GI obstruction recommended.

underlined – top prescribed drug


HYDROcodone 567

INTERACTIONS Dosage in Hepatic Impairment


DRUG: CNS depressants (e.g., alcohol, Use caution.
morphine, oxyCODONE, zolpidem) SIDE EFFECTS
may increase CNS depression. MAOIs
(e.g., phenelzine, selegiline) may in- Frequent: Lethargy, hypotension, dia-
crease adverse effects. CYP3A4 inhibitors phoresis, facial flushing, dizziness,
(e.g., clarithromycin, ketoconazole, drowsiness. Occasional: Urine retention,
ritonavir) may increase or prolong opioid blurred vision, constipation, dry mouth,
effects. HERBAL: Herbals with sedative headache, nausea, vomiting, difficult/
properties (e.g., chamomile, kava, painful urination, euphoria, dysphoria.
kava, valerian) may increase CNS de-
pression. St. John’s wort may decrease ADVERSE EFFECTS/TOXIC
concentration/effect. FOOD: None known. REACTIONS
LAB VALUES: May increase serum amy- Overdose results in respiratory depres- H
lase, lipase. sion, skeletal muscle flaccidity, cold/
clammy skin, cyanosis, extreme drowsi-
AVAILABILITY (Rx) ness progressing to seizures, stupor,
coma. Tolerance to analgesic effect,
Capsules: (Extended-Release [Zo- physical dependence may occur with re-
hydro ER]): 10 mg, 15 mg, 20 mg, 30 mg, peated use. Prolonged duration of action,
40 mg, 50 mg. Tablets: (Extended-Release cumulative effect may occur in those with
[Hysingla ER]): 20 mg, 30 mg, 40 mg, 60 hepatic/renal impairment. Antidote:
mg, 80 mg, 100 mg, 120 mg. Naloxone (see Appendix J).
ADMINISTRATION/HANDLING NURSING CONSIDERATIONS
PO BASELINE ASSESSMENT
• Give without regard to food. • Ex-
tended-release capsules/tablets must be Obtain vital signs. If respirations are 12/
swallowed whole. Do not cut, crush, or min or less (20/min or less in children),
dissolve. withhold medication, contact physician.
Analgesic: Assess onset, type, location,
INDICATIONS/ROUTES/DOSAGE duration of pain. Effect of medication is
reduced if full pain recurs before next
Analgesia (Combination Products) dose. Antitussive: Assess type, severity,
PO: ADULTS, CHILDREN WEIGHING 50 KG frequency of cough.
OR MORE: Initially, 2.5–10 mg q3–4h as
needed. ADULTS, CHILDREN WEIGHING LESS INTERVENTION/EVALUATION
THAN 50 KG: Initially, 0.1–0.2 mg/kg q4–
Palpate bladder for urinary retention.
6h as needed. ELDERLY: 2.5–5 mg q4–6h. Monitor daily pattern of bowel activity,
Analgesia (Extended-Release)
stool consistency. Initiate deep breathing
PO: ADULTS, ELDERLY: (Zohydro ER): Ini-
and coughing exercises, particularly in
tially, 10 mg q12h. May increase by 10 mg pts with pulmonary impairment. Assess
q12h q3–7 days to achieve adequate anal- for clinical improvement; record onset of
gesia. (Hysingla ER): Initially, 20 mg q24h. relief of pain, cough. Monitor LOC.
May titrate in increments of 10–20 mg PATIENT/FAMILY TEACHING
q3–5 days to achieve adequate analgesia.
• Go from lying to standing slowly to
Dosage in Renal Impairment avoid orthostatic hypotension. • Avoid
No dose adjustment. tasks that require alertness, motor skills

Canadian trade name Non-Crushable Drug High Alert drug


568 hydrocortisone
until response to drug is estab- d­ ysfunction, cirrhosis, hypertension, os-
lished. • Avoid alcohol. • Tolerance teoporosis, thromboembolic tendencies
or dependence may occur with pro- or thrombophlebitis, HF, seizure disor-
longed use at high dosages. • Report ders, diabetes, respiratory tuberculosis,
nausea, vomiting, constipation, shortness untreated systemic infections, renal/he-
of breath, difficulty breathing. patic impairment, acute MI, myasthenia
gravis, glaucoma, cataracts, increased
intraocular pressure, elderly, immuno-
compromised pts (e.g., diabetes, renal
hydrocortisone failure, open wounds).

hye-droe-kor-ti-sone ACTION
(Anusol HC, Caldecort, Colocort, Inhibits accumulation of inflammatory
H Cortaid, SOLU-Cortef, Cortenema, Cor- cells at inflammation sites, phagocytosis,
tizone-10, Preparation H Hydrocorti- lysosomal enzyme release, synthesis and/
sone, Proctocort, Westcort, Cortef) or release of mediators of inflammation.
Do not confuse hydrocortisone Reverses increased capillary permeabil-
with hydroCHLOROthiazide, ity. Therapeutic Effect: Prevents/sup-
HYDROcodone, or hydroxychlo- presses cell-mediated immune reactions.
roquine, Cortef with Coreg, or Decreases/prevents tissue response to
SOLU-Cortef with SOLU-medrol. inflammatory process.
FIXED-COMBINATION(S) PHARMACOKINETICS
Cortisporin: hydrocortisone/neomy- Route Onset Peak Duration
cin/polymyxin (an anti-infective): 5 IV N/A 4–6 hrs 8–12 hrs
mg/10,000 units/5 mg, 10 mg/10,000
units/5 mg. Lipsovir: hydrocortisone/ Well absorbed after IM administration.
acyclovir (an antiviral): 1%/5%. Widely distributed. Metabolized in liver.
Half-life: Plasma, 1.5–2 hrs; biologic,
uCLASSIFICATION 8–12 hrs.
PHARMACOTHERAPEUTIC: Corticos-
teroid. CLINICAL: Glucocorticoid. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses pla-
centa; distributed in breast milk. May
USES produce cleft palate if used chronically
Systemic: Management of adrenocorti- during first trimester. Breastfeeding not
cal insufficiency, anti-inflammatory, im- recommended. Children: Prolonged
munosuppressive. Topical: Inflamma- treat­ment or high dosages may decrease
tory dermatoses, adjunctive treatment short-term growth rate, cortisol secre-
of ulcerative colitis, atopic dermatitis, tion. Elderly: May be more susceptible
inflamed hemorrhoids. OFF-LABEL: Man- to developing hypertension or osteopo-
agement of septic shock. Treatment of rosis.
thyroid storm.
INTERACTIONS
PRECAUTIONS DRUG: May increase hypokalemic ef-
Contraindications: Hypersensitivity to hy- fects of diuretics (e.g., furosemide).
drocortisone. Systemic fungal infections. CYP3A4 inducers (e.g., carBAM-
Use in premature infants. Administration azepine, phenytoin, rifAMPin) may
of live or attenuated virus vaccines. IM decrease effects. Live virus vaccines
administration in idiopathic thrombo- may decrease pt’s antibody response to
cytopenia purpura. Cautions: Thyroid vaccine, increase vaccine side effects,

underlined – top prescribed drug


hydrocortisone 569
potentiate virus replication. May de- left leg extended, right leg flexed. • Gen-
crease therapeutic effect of aldesleukin, tly insert applicator tip into rectum,
BCG (intravesical). May increase hy- pointed slightly toward navel (umbili-
ponatremic effect of desmopressin. cus). Slowly instill medication.
HERBAL: St. John’s wort may decrease
concentration. Echinacea may decrease Topical
therapeutic effect. FOOD: None known. • Gently cleanse area before applica-
LAB VALUES: May increase serum glu- tion. • Use occlusive dressings only as
cose, lipids, sodium. May decrease se- ordered. • Apply sparingly; rub into
rum calcium, potassium, thyroxine; WBC area thoroughly.
count.
IV INCOMPATIBILITIES
AVAILABILITY (Rx) Ciprofloxacin (Cipro), diazePAM (Va-
Cream, Rectal: (Cortizone-10, Preparation lium), midazolam (Versed), phenytoin H
H Hydrocortisone): 1%, 2.5%. Cream, (Dilantin).
Topical: 0.5%, 1%, 2.5%. Injection, Pow-
der for Reconstitution: (Solu-Cortef): 100 IV COMPATIBILITIES
mg, 250 mg, 500 mg, 1 g. Ointment, Amphotericin, calcium gluconate, ce-
Topical: 0.5%, 1%, 2.5%. Suppository
fepime (Maxipime), digoxin (Lanoxin),
(Anusol HC): 25 mg. Suspension, Rectal:
dilTIAZem (Cardizem), diphenhydrAMINE
(Colocort, Cortenema): 100 mg/60 mL.
(Benadryl), DOPamine (Intropin), insu-
Tablets: (Cortef): 5 mg, 10 mg, 20 mg.
lin, lidocaine, LORazepam (Ativan), mag-
ADMINISTRATION/HANDLING nesium sulfate, morphine, norepinephrine
(Levophed), procainamide (Pronestyl),
IV potassium chloride, propofol (Diprivan).
Hydrocortisone Sodium Succinate
Reconstitution • Initially, reconsti- INDICATIONS/ROUTES/
tute vial per manufacturer’s instruc- DOSAGE
tions. • May further dilute with D5W or Acute Adrenal Insufficiency
0.9% NaCl. For IV push, dilute to 50 mg/ IV: ADULTS, ELDERLY: 100 mg IV bo-
mL; for intermittent infusion, dilute to 1 lus, then 25–75 mg q6h for 24 hrs (or
mg/mL. Note: 100–3,000 mg may be 200 mg/24h as continuous infusion),
added to 50 mL D5W or 0.9% NaCl. then taper slowly. INFANTS, CHILDREN,
Rate of administration • Administer ADOLESCENTS: 50–100 mg/m2 once, then
IV push over 3–5 min (over 10 min for 50–100 mg/m2/day in 4 divided doses.
doses 500 mg or greater). Give intermit-
tent infusion over 20–30 min. Anti-inflammation, Immunosuppression
Storage • Store at room tempera- IV, IM: ADULTS, ELDERLY: 100–500 mg/
ture. • Once reconstituted, stable for 3 dose at intervals of 2 hrs, 4 hrs, or 6 hrs.
days at room temperature. Once further CHILDREN: 1–5 mg/kg/day in divided
diluted with 0.9% NaCl or D5W, stability is doses q12h.
concentration dependent: 1 mg/mL (24 PO: ADULTS, ELDERLY: 20–240 mg
hrs), 2–60 mg/mL (4 hrs). q12h. CHILDREN: 2.5–10 mg/kg/day in
divided doses q6–8h.
PO
• Give with food or milk if GI distress Adjunctive Treatment of Ulcerative
occurs. Colitis
Rectal: (Enema): ADULTS, ELDERLY: 100
Rectal mg at bedtime for 21 nights or until clini-
• Shake homogeneous suspension cal and proctologic remission occurs
well. • Instruct pt to lie on left side with (may require 2–3 mos of therapy).
Canadian trade name Non-Crushable Drug High Alert drug
570 HYDROmorphone
(Rectal Foam): ADULTS, ELDERLY: 1 ap- daily pattern of bowel activity, stool
plicator 1–2 times/day for 2–3 wks, then consistency. Monitor electrolytes, B/P,
every second day until therapy ends. weight, serum glucose. Monitor for hy-
pocalcemia (muscle twitching, cramps),
Usual Topical Dose hypokalemia (weakness, paresthesia
ADULTS, ELDERLY: Apply sparingly 2–4 [esp. lower extremities], nausea/vomit-
times/day. ing, irritability, ECG changes). Assess
emotional status, ability to sleep.
Dosage in Renal/Hepatic Impairment
No dose adjustment. PATIENT/FAMILY TEACHING
• Report fever, sore throat, muscle aches,
SIDE EFFECTS sudden weight gain, swelling, visual distur-
Frequent: Insomnia, heartburn, anxiety, bances, behavioral changes. • Do not take
H abdominal distention, diaphoresis, acne, aspirin or any other medication without
mood swings, increased appetite, facial consulting physician. • Limit caffeine;
flushing, delayed wound healing, increased avoid alcohol. • Inform dentist, other phy-
susceptibility to infection, diarrhea or con- sicians of cortisone therapy now or within
stipation. Occasional: Headache, edema, past 12 mos. • Caution against overusing
change in skin color, frequent urination. joints injected for symptomatic re-
Topical: Pruritus, redness, irritation. lief. • Topical: Apply after shower or bath
Rare: Tachycardia, allergic reaction (rash, for best absorption. • Do not cover or use
hives), psychological changes, hallucina- occlusive dressings unless ordered by physi-
tions, depression. Topical: Allergic contact cian; do not use tight diapers, plastic pants,
dermatitis, purpura. Systemic: Absorption coverings. • Avoid contact with eyes.
more likely with use of occlusive dressings
or extensive application in young children.
ADVERSE EFFECTS/TOXIC HYDROmorphone
REACTIONS
Long-term therapy: Hypocalcemia, hy- hye-droe-mor-fone
pokalemia, muscle wasting (esp. arms, (Dilaudid, Exalgo, Hydromorph
legs), osteoporosis, spontaneous fractures, Contin )
amenorrhea, cataracts, glaucoma, pep- j BLACK BOX ALERT jHigh abuse
tic ulcer, HF. Abrupt withdrawal after potential, life-threatening respiratory
depression risk. Other opioids, alco-
long-term therapy: Nausea, fever, head- hol, CNS depressants increase risk
ache, sudden severe joint pain, rebound of potentially fatal respiratory de-
inflammation, fatigue, weakness, lethargy, pression. Highly concentrated form
dizziness, orthostatic hypotension. (Dilaudid HP, 10 mg/mL) not to be
interchanged with less concentrated
NURSING CONSIDERATIONS form (Dilaudid); overdose, death may
result. Exalgo: For use in opioid-tol-
BASELINE ASSESSMENT erant pts. Do not crush, break, chew,
or dissolve. Swallow whole.
Obtain baseline weight, B/P, serum glu-
Do not confuse Dilaudid with
cose, cholesterol, electrolytes. Screen for
Demerol or Dilantin, or HY-
infections including fungal infections, TB,
DROmorphone with HYDROco-
viral skin lesions. Question medical his-
done or morphine.
tory as listed in Precautions.
INTERVENTION/EVALUATION uCLASSIFICATION
Assess for edema. Be alert to infec- PHARMACOTHERAPEUTIC: Opioid
tion (reduced immune response): sore agonist (Schedule II). CLINICAL:
throat, fever, vague symptoms. M
­ onitor Narcotic analgesic.

underlined – top prescribed drug


HYDROmorphone 571

USES milk. May prolong labor if administered


Relief of moderate to severe pain. Extended- in latent phase of first stage of labor or
release tablet (Exalgo): Around the clock, before cervical dilation of 4–5 cm has oc-
continuous analgesia for extended period. curred. Respiratory depression may oc-
cur in neonate if mother receives opiates
PRECAUTIONS during labor. Regular use of opiates dur-
ing pregnancy may produce withdrawal
Contraindications: Hypersensitivity to HY-
symptoms in the neonate (irritability,
DROmorphone. Acute or severe bronchial
excessive crying, tremors, hyperactive
asthma, severe respiratory depression.
reflexes, fever, vomiting, diarrhea, yawn-
GI obstruction including paralytic ileus
ing, sneezing, seizures). Children: Pts
(known or suspected). Additional Prod-
younger than 2 yrs may be more sus-
uct-Specific Contraindications: Dilaudid
ceptible to respiratory depression. El-
HP injection: Opioid-intolerant pts. H
derly: May be more susceptible to respi-
Extended-Release Tablets: Opioid-­
ratory depression, may cause paradoxical
intolerant pts, preexisting GI surgery/
excitement. Age-related renal impairment,
diseases causing GI narrowing. Cau-
prostatic hypertrophy or obstruction may
tions: Severe hepatic, renal, respiratory
increase risk of urinary retention; dosage
disease; hypothyroidism, adrenal cortical
adjustment recommended.
insufficiency, seizures, acute alcoholism,
head injury, intracranial lesions, increased INTERACTIONS
intracranial pressure, prostatic hypertro-
DRUG: CNS depressants (e.g., al-
phy, Addison’s disease, urethral stricture,
cohol, morphine, oxyCODONE,
pancreatitis, biliary tract disease, cardio-
zolpidem) may increase CNS depres-
vascular disease, morbid obesity, delirium
sion. MAOIs (e.g., phenelzine, sele-
tremens, toxic psychosis, pts with CNS de-
giline) may increase adverse effects.
pression or coma, pts with depleted blood
HERBAL: Herbals with sedative prop-
volume, obstructive bowel disorder.
erties (e.g., chamomile, kava, kava,
ACTION valerian) may increase CNS depression.
FOOD: None known. LAB VALUES: May
Binds to opioid receptors in CNS, reduc-
increase serum amylase, lipase.
ing intensity of pain stimuli from sensory
nerve endings. Therapeutic Effect: Al- AVAILABILITY (Rx)
ters perception, emotional response to
Injection, Solution: 1 mg/mL, 2 mg/mL,
pain; suppresses cough reflex.
4 mg/mL, 10 mg/mL. Liquid, Oral: 1 mg/
PHARMACOKINETICS mL. Suppository: 3 mg. Tablets: 2 mg, 4
mg, 8 mg.
Route Onset Peak Duration
Tablets: (Extended-Release [Exalgo]):
PO 30 min 90–120 min 4 hrs
IV 10–15 min 15–30 min 2–3 hrs 8 mg, 12 mg, 16 mg, 32 mg.
IM 15 min 30–60 min 4–5 hrs
SQ 15 min 30–90 min 4 hrs ADMINISTRATION/HANDLING
Rectal 15–30 min N/A N/A IV
Well absorbed from GI tract after IM ad- b ALERT c High-concentration injection
ministration. Widely distributed. Metabo- (10 mg/mL) should be used only in pts
lized in liver. Excreted in urine. Half- tolerant to opiate agonists, currently re-
life: 2.6–4 hrs. ceiving high doses of another opiate ago-
nist for severe, chronic pain due to cancer.
LIFESPAN CONSIDERATIONS Reconstitution • May give undi-
Pregnancy/Lactation: Readily crosses luted. • May further dilute with 5 mL
placenta. Unknown if distributed in breast Sterile Water for Injection or 0.9% NaCl.
Canadian trade name Non-Crushable Drug High Alert drug
572 HYDROmorphone
Rate of administration • Administer INDICATIONS/ROUTES/DOSAGE
IV push very slowly (over 2–3 Analgesia (Acute, Moderate to Severe)
min). • Rapid IV increases risk of se- PO: ADULTS: (Immediate-Release):
vere adverse reactions (chest wall rigid- Initially 2–4 mg q4–6h as needed (tablets)
ity, apnea, peripheral circulatory col- or 2.5–10 mg q3–6h as needed (liquid).
lapse, anaphylactoid effects, cardiac ELDERLY: Use with caution; initiating at the
arrest). low end of the dosage range is recom-
Storage • Store at room temperature; mended. CHILDREN, ADOLESCENTS WEIGH-
protect from light. • Slight yellow dis- ING MORE THAN 50 KG: 1–2 mg q3–4h
coloration of parenteral form does not as needed. CHILDREN OLDER THAN 6 MOS
indicate loss of potency. WEIGHING LESS THAN 50 KG: 0.03–0.08 mg/
kg/dose q3–4h as needed.
IM, SQ
IV (For use in opiate-naive pts):
H • Subcutaneously or intramuscularly
ADULTS, ELDERLY: 0.2–1 mg q2–3h (pts with
insert needle and inject solution. Pulling
prior opioid exposure may require higher
back the plunger before IM injection may
doses). CHILDREN, ADOLESCENTS WEIGHING
ensure that drug is not delivered directly
MORE THAN 50 KG: 0.2–0.6 mg/dose q2–
into bloodstream (however, this topic is
4h as needed. CHILDREN WEIGHING 50 KG OR
currently debated). • Administer slowly;
LESS: 0.015 mg/kg/dose q3–6h as needed.
rotate injection sites. • Pts with circula-
Rectal: ADULTS, ELDERLY: 3 mg q6–8h.
tory impairment experience higher risk
of overdosage due to delayed absorption Patient-Controlled Analgesia (PCA)
of repeated administration. IV: ADULTS, ELDERLY: (Usual concentra-
tion: 0.2 mg/mL). Demand dose: Initially,
PO
0.1–0.2 mg. Range: 0.05–0.4 mg. Lock-
• Give without regard to food. • Tab-
out interval: 6 min. Range: 5–10 min.
lets may be crushed. • Extended-­
Epidural: ADULTS, ELDERLY: Bolus dose
release tablets must be swallowed whole;
of 0.4–1 mg; infusion rate: 0.03–0.3 mg/
do not break, crush, dissolve, or divide.
hr; demand dose: 0.02–0.05 mg. Lock-
Rectal out interval: 10–15 min.
• Refrigerate suppositories. • Moisten
Continuous Infusion
suppository with cold water before in-
IV infusion: ADULTS, ELDERLY: 0.5–3
serting well up into rectum.
mg/hr.
IV INCOMPATIBILITIES
Dosage in Renal/Hepatic Impairment
Amphotericin B complex (Abelcet, Am- Decrease initial dose; use with caution.
Bisome, Amphotec), ceFAZolin (Ancef,
Kefzol), diazePAM (Valium), PHENobar- SIDE EFFECTS
bital, phenytoin (Dilantin). Frequent: Drowsiness, dizziness, hypoten-
sion (including orthostatic hypotension),
IV COMPATIBILITIES
decreased appetite. Occasional: Confu-
Dexmedetomidine (Precedex), dilTIAZem sion, diaphoresis, facial flushing, urinary
(Cardizem), diphenhydrAMINE (Bena- retention, constipation, dry mouth, nau-
dryl), DOBUTamine (Dobutrex), DOPa- sea, vomiting, headache, pain at injection
mine (Intropin), fentaNYL (Sublimaze), site. Rare: Allergic reaction, depression.
furosemide (Lasix), heparin, LORazepam
(Ativan), magnesium sulfate, metoclo- ADVERSE EFFECTS/TOXIC
pramide (Reglan), midazolam (Versed), REACTIONS
milrinone (Primacor), morphine, propo- Overdose results in respiratory depres-
fol (Diprivan). sion, skeletal muscle flaccidity, cold/

underlined – top prescribed drug


hydrOXYzine 573
clammy skin, cyanosis, extreme drowsi- Do not confuse hydrOXYzine
ness progressing to seizures, stupor, with hydrALAZINE or hydroxyu-
coma. Tolerance to analgesic effect, rea, or Vistaril with Restoril,
physical dependence may occur with Versed, or Zestril.
repeated use. Prolonged duration of
action, cumulative effect may occur in uCLASSIFICATION
those with hepatic/renal impairment. PHARMACOTHERAPEUTIC: Hista-
Antidote: Naloxone (see Appendix J). mine H1 antagonist. CLINICAL: Anti-
histamine, antianxiety, antispasmod-
NURSING CONSIDERATIONS ic, antiemetic, antipruritic.
BASELINE ASSESSMENT
Obtain vital signs. If respirations are 12/ USES
min or less (20/min or less in children), Antiemetic, treatment of anxiety/agita- H
withhold medication, contact physician. tion, antipruritic.
Analgesic: Assess onset, type, location,
duration of pain. Effect of medication is PRECAUTIONS
reduced if full pain recurs before next Contraindications: Hypersensitivity to hy-
dose. Antitussive: Assess type, severity, drOXYzine. Early pregnancy; SQ, IV admin-
frequency of cough. istration; pts with prolonged QT interval.
Cautions: Narrow-angle glaucoma, pros-
INTERVENTION/EVALUATION
tatic hypertrophy, bladder neck obstruc-
Monitor vital signs; assess for pain relief, tion, asthma, COPD, elderly.
cough. To prevent pain cycles, instruct
pt to request pain medication as soon as ACTION
discomfort begins. Monitor daily pattern Competes with histamine for receptor
of bowel activity, stool consistency (esp. sites in GI tract, blood vessels, respira-
in long-term use). Initiate deep breath- tory tract. Therapeutic Effect: Pro-
ing and coughing exercises, particularly duces anxiolytic, anticholinergic, antihis-
in pts with pulmonary impairment. Assess taminic, analgesic effects; relaxes skeletal
for clinical improvement; record onset of muscle; controls nausea, vomiting.
relief of pain, cough.
PHARMACOKINETICS
PATIENT/FAMILY TEACHING
Route Onset Peak Duration
• Avoid alcohol. • Avoid tasks that re- PO 15–30 min N/A 4–6 hrs
quire alertness/motor skills until re-
sponse to drug is established. • Toler- Well absorbed from GI tract and after
ance or dependence may occur with parenteral administration. Metabolized
prolonged use at high dosages. • in liver. Primarily excreted in urine.
Change positions slowly to avoid ortho- Not removed by hemodialysis. Half-
static hypotension. • Do not chew, life: 3–7 hrs (increased in elderly, he-
crush, dissolve, or divide extended-­ patic impairment).
release tablets.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if drug
crosses placenta or is distributed in
hydrOXYzine breast milk. Children: Not recom-
mended in newborns or premature in-
hye-drox-ee-zeen fants (increased risk of anticholinergic
(Apo-HydrOXYzine , Atarax , effects). Paradoxical excitement may oc-
Novo-Hydroxyzin , Vistaril) cur. Elderly: Increased risk of ­dizziness,

Canadian trade name Non-Crushable Drug High Alert drug


574 hydrOXYzine
sedation, confusion. Hypotension, hyper- Dosage in Renal/Hepatic Impairment
excitability may occur. No dose adjustment. Change dosing in-
terval to q24h in pts with primary biliary
INTERACTIONS cirrhosis.
DRUG: QT interval–prolonging medi-
cations (e.g., amiodarone, azithro- SIDE EFFECTS
mycin, ceritinib, haloperidol, Side effects are generally mild, tran-
moxifloxacin) may increase risk of sient. Frequent: Drowsiness, dry mouth,
QT interval prolongation, torsades de marked discomfort with IM injection.
pointes. CNS depressants (e.g., al- Occasional: Dizziness, ataxia, asthenia,
cohol, morphine, oxyCODONE, zol- slurred speech, headache, agitation, in-
pidem) may increase CNS depression. creased anxiety. Rare: Paradoxical reac-
Aclidinium, ipratropium, tiotro- tions (hyperactivity, anxiety in children;
H pium, umeclidinium may increase excitement, restlessness in elderly or de-
anticholinergic effect. HERBAL: Herb- bilitated pts) generally noted during first
als with sedative properties (e.g., 2 wks of therapy, particularly in presence
chamomile, kava, kava, vale- of uncontrolled pain.
rian) may increase CNS depression.
FOOD: None known. LAB VALUES: May ADVERSE EFFECTS/TOXIC
cause false-positive urine 17-hydroxy- REACTIONS
corticosteroid determinations. Hypersensitivity reaction (wheezing, dys-
pnea, chest tightness) may occur. QT in-
AVAILABILITY (Rx) terval prolongation, torsades de pointes
Oral Solution: 10 mg/5 mL. Syrup: 10 have been reported. Acute generalized
mg/5 mL. Tablets: 10 mg, 25 mg, 50 mg. exanthematous pustulosis (AGEP) may
Capsules: 25 mg, 50 mg, 100 mg. occur.

ADMINISTRATION/HANDLING NURSING CONSIDERATIONS


PO BASELINE ASSESSMENT
• May give without regard to food. • Anxiety: Offer emotional support. Assess
Shake oral suspension well. • Scored motor responses (agitation, trembling,
tablets may be crushed; do not break, tension), autonomic responses (cold/
crush, or open capsule. clammy hands, diaphoresis). Anti-
emetic: Assess for dehydration (poor
INDICATIONS/ROUTES/DOSAGE skin turgor, dry mucous membranes,
Anxiety longitudinal furrows in tongue).
Note: Initiate elderly dose at the lower
end of recommended dosage. INTERVENTION/EVALUATION
PO: ADULTS, ELDERLY: 50–100 mg 4 For pts on long-term therapy, CBC, BMP,
times/day or 37.5–75 mg/day in divided LFT should be performed periodically.
doses. CHILDREN 6 YRS AND OLDER: 12.5– Monitor lung sounds for signs of hy-
25 mg 3–4 times/day. CHILDREN YOUNGER persensitivity reaction. Monitor serum
THAN 6 YRS: 12.5 mg 3–4 times/day. electrolytes in pts with severe vomiting.
Assess for paradoxical reaction, particu-
Pruritus larly during early therapy. Assist with am-
PO: ADULTS, ELDERLY: 25 mg 3–4 times/ bulation if drowsiness, light-headedness
day. CHILDREN 6 YRS AND OLDER: 12.5–25 occur. Obtain ECG if palpitations occur
mg 3–4 times/day. CHILDREN YOUNGER or cardiac arrhythmia is suspected. As-
THAN 6 YRS: 12.5 mg 3–4 times/day. sess skin for rash, pustules.

underlined – top prescribed drug


hydrOXYzine 575
PATIENT/FAMILY TEACHING drug is established. • Treatment may
• Marked discomfort may occur with IM cause life-threatening heart arrhythmias;
injection. • Sugarless gum, sips of wa- report chest pain, difficulty breathing,
ter may relieve dry mouth. • Drowsi- palpitations, passing out. Do not take
ness usually diminishes with continued newly prescribed medications unless ap-
therapy. • Avoid tasks that require proved by prescriber who originally
alertness, motor skills until response to started treatment.

Canadian trade name Non-Crushable Drug High Alert drug


576 ibalizumab-uiyk
LIFESPAN CONSIDERATIONS
ibalizumab-uiyk Pregnancy/Lactation: Breastfeeding
not recommended due to risk of post-
i-ba-liz-ue-mab-uiyk natal HIV transmission. Unknown if dis-
(Trogarzo) tributed in breast milk. However, human
Do not confuse ibalizumab with immunoglobulin G (IgG) is present in
atezolizumab, benralizumab, breast milk and is known to cross the
certolizumab, daclizumab, placenta. Children: Safety and efficacy
eculizumab, efalizumab, not established. Elderly: No age-related
ibritumomab, ipilimumab, precautions noted.
mepolizumab, ocrelizumab,
pembrolizumab, tocilizumab, INTERACTIONS
or vedolizumab. DRUG: May enhance adverse/toxic effect
uCLASSIFICATION of belimumab. HERBAL: None significant.
FOOD: None known. LAB VALUES: May
I PHARMACOTHERAPEUTIC: CD4-­ increase serum bilirubin, creatinine, glu-
directed post-attachment HIV-1 inhib- cose, lipase, uric acid. May decrease Hgb,
itor. Monoclonal antibody. CLINICAL: platelets, leukocytes, neutrophils.
Antiviral (anti-HIV).
AVAILABILITY (Rx)
Injection Solution: 200 mg/1.33 mL
USES (150 mg/mL).
Treatment of HIV-1 infection, in combina- ADMINISTRATION/HANDLING
tion with other antiretrovirals, in heavily
treatment-experienced adults with multi- IV
drug-resistant HIV-1 infection who are fail- Preparation • Calculate the number of
ing their current antiretroviral regimen. vials needed for each dose. • Visually
inspect for particulate matter or discolor-
PRECAUTIONS ation. Solution should appear clear to
Contraindications: Hypersensitivity to slightly opalescent and colorless to slightly
ibalizumab. Cautions: Baseline anemia, yellow in color. Do not use if solution is
leukopenia, neutropenia, thrombocyto- cloudy or discolored or if visible particles
penia. Pt at risk for hyperglycemia (e.g., are observed. • Dilute in 250 mL 0.9%
diabetes, recent surgery, chronic use of NaCl (do not dilute in other solutions).
corticosteroids). Administration guidelines • Recom-
mend infusion into cephalic vein of right
ACTION or left arm. If cephalic vein cannot be
Selectively binds to domain 2 of CD4+, used, an appropriate vein located else-
inhibiting post-attachment steps required where may be utilized. • Once infusion
for entry of HIV-1 virus particles into host is complete, flush with 30 mL of 0.9%
cells. Blocks HIV-1 from infecting CD4+T NaCl.
cells without causing immunosuppression Rate of administration • Infuse load-
or depleting CD4+ cell counts. Therapeu- ing dose over at least 30 min (or more). If
tic Effect: Interferes with HIV replication, no infusion-related reactions occur, may
slowing progression of HIV infection. infuse maintenance doses over at least 15
min (or more). • Do not infuse as IV
PHARMACOKINETICS push or bolus.
Widely distributed. Metabolism not speci- Storage • Refrigerate unused vials.
fied. Steady state reached after first main- • Do not freeze. • Protect from light.
tenance dose. Excretion not specified. • May refrigerate diluted solution for up to
Half-life: 2.7–64 hrs. 24 hrs or store at room temperature for no
underlined – top prescribed drug
ibandronate 577
more than 4 hrs. • If refrigerated, allow INTERVENTION/EVALUATION
diluted solution to warm to room tempera- Periodically monitor CBC for anemia, leu-
ture for at least 30 min before infusion. kopenia, neutropenia, thrombocytopenia;
serum bilirubin. Monitor CD4+ count, viral
INDICATIONS/ROUTES/DOSAGE load, HIV-1 RNA level for treatment effec-
HIV-1 Infection (Heavily Treatment- tiveness. After loading dose is given, moni-
Experienced) tor all pts for infusion-related reactions for
IV: ADULTS, ELDERLY: Loading dose of at least 1 hr. If no infusion-related reactions
2,000 mg once. Maintenance: 800 mg have occurred, may decrease postinfusion
q2wks. If a maintenance dose is missed observation time to 15 min for subsequent
by 3 days or more, readminister load- infusions. Monitor daily pattern of bowel
ing dose. Then, reschedule maintenance activity, stool consistency; I&Os.
doses q2wks thereafter.
PATIENT/FAMILY TEACHING
Dosage in Renal/Hepatic Impairment
• Treatment does not cure HIV infection
Mild to severe impairment: Not speci- I
nor reduce risk of transmission. Practice
fied; use caution. safe sex with barrier methods or absti-
SIDE EFFECTS nence. • As immune system strengthens,
it may respond to dormant infections hid-
Occasional (8%–5%): Diarrhea, dizziness, den within the body. Report any new fever,
nausea, rash (erythematous, generalized, chills, body aches, cough, night sweats,
macular, maculopapular, papular). shortness of breath. • All pts must be ob-
ADVERSE EFFECTS/TOXIC served for infusion reactions during infu-
REACTIONS sion and after infusion is completed.
• Treatment may depress your immune
Anemia, leukopenia, neutropenia, thrombo- system response and reduce your ability to
cytopenia are expected responses to therapy. fight infection. Report symptoms of infec-
May induce immune reconstitution syn- tion such as body aches, chills, cough,
drome (inflammatory response to dormant ­fatigue, fever. Avoid those with active infec-
opportunistic infections, such as Mycobac- tion. • Do not breastfeed. • Report
terium avium, cytomegalovirus, PCP, or symptoms of elevated blood sugar levels
tuberculosis, or acceleration of autoimmune (blurred vision, headache, increased thirst,
disorders, such as Graves’ disease, polymyo- frequent urination).
sitis, Guillain-Barré). Immunogenicity (auto-
ibalizumab antibodies) occurs rarely. Hyper-
glycemia (serum blood glucose greater than
250 mg/dL) reported in 3% of pts. ibandronate
NURSING CONSIDERATIONS
eye-ban-droe-nate
BASELINE ASSESSMENT (Boniva)
Obtain CBC, CD4+ count, viral load, uCLASSIFICATION
HIV-1 RNA level. Verify that pt is heavily
treatment-experienced with multidrug PHARMACOTHERAPEUTIC: Bisphos-
resistance and failing their current HIV-1 phonate. CLINICAL: Calcium regulator.
antiretroviral regimen. Question history
of diabetes, hyperglycemia. Assess usual USES
bowel movement patterns, stool char- Treatment/prevention of osteoporosis in
acteristics. Screen for active infection. postmenopausal women. OFF-LABEL: Hy-
Question history of infusion-related reac- percalcemia of malignancy; reduces bone
tions before each infusion. pain and skeletal complications from met-
astatic bone disease due to breast cancer.
Canadian trade name Non-Crushable Drug High Alert drug
578 ibandronate
PRECAUTIONS ADMINISTRATION/HANDLING
Contraindications: Hypersensitivity to PO
ibandronate, other bisphosphonates; oral • Give 60 min before first food or bever-
tablets in pts unable to stand or sit upright age of the day, on an empty stomach with
for at least 60 min; pts with abnormalities 6–8 oz plain water (not mineral water)
of the esophagus that would delay emptying while pt is standing or sitting in upright
(e.g., stricture, achalasia), hypocalcemia. position. • Pt cannot lie down for 60
Cautions: GI diseases (duodenitis, dys- min following administration. • In-
phagia, esophagitis, gastritis, ulcers [drug struct pt to swallow whole; do not break,
may exacerbate these conditions]), renal crush, dissolve, or divide tablet (poten-
impairment with CrCl less than 30 mL/min. tial for oropharyngeal ulceration).
ACTION IV
Inhibits bone resorption via activity on os- • Give over 15–30 sec. • Give over 1
teoclasts. Therapeutic Effect: Reduces hr for metastatic bone disease; over 1–2
I rate of bone resorption, resulting in indi- hrs for hypercalcemia of malignancy.
rect increased bone mineral d­ ensity.
INDICATIONS/ROUTES/DOSAGE
PHARMACOKINETICS Note: May consider discontinuing after
Absorbed in upper GI tract. Extent of 3–5 yrs in pts at low risk for fracture.
absorption impaired by food, beverages Consider supplemental calcium and vita-
(other than plain water). Protein bind- min D if dietary intake is inadequate.
ing: 85%–99%. Rapidly binds to bone.
Unabsorbed portion excreted in urine. Osteoporosis
Half-life: PO: 37–157 hrs; IV: 5–25 PO (Prevention/Treatment): ADULTS,
hrs. ELDERLY: 150 mg once monthly.
IV (Treatment): ADULTS, ELDERLY: 3 mg
LIFESPAN CONSIDERATIONS q3mos.
Pregnancy/Lactation: May cause fetal
harm/malformations. Unknown if distrib- Dosage in Renal Impairment
uted in breast milk. Breastfeeding not Not recommended for pts with CrCl less
recommended. Children: Safety and ef- than 30 mL/min.
ficacy not established. Elderly: No age- Dosage in Hepatic Impairment
related precautions noted. No dose adjustment.
INTERACTIONS SIDE EFFECTS
DRUG: Antacids, calcium, magnesium Frequent (13%–6%): Back pain, dyspep-
may decrease concentration/effect. Aspirin, sia, peripheral discomfort, diarrhea,
NSAIDs (e.g., ibuprofen, ketorolac, headache, myalgia. IV: Abdominal pain,
naproxen) may increase adverse effects. dyspepsia, constipation, nausea, diar-
HERBAL: None significant. FOOD: Bever-
rhea. Occasional (4%–3%): Dizziness,
ages (other than plain water), dietary arthralgia, asthenia. Rare (2% or
supplements, dairy products, food in- less): Vomiting, hypersensitivity reaction.
terfere with absorption. LAB VALUES: May
decrease serum alkaline phosphatase. May ADVERSE EFFECTS/TOXIC
increase serum cholesterol. REACTIONS
AVAILABILITY (Rx) Upper respiratory infection occurs occasion-
ally. Overdose results in hypocalcemia, hypo-
Injection Solution: 3 mg/3 mL syringe. phosphatemia, significant GI disturbances.
Tablets: 150 mg.

underlined – top prescribed drug


ibrutinib 579

NURSING CONSIDERATIONS USES


Treatment of pts with mantle cell lymphoma
BASELINE ASSESSMENT (MCL) who have received at least one prior
Hypocalcemia, vitamin D deficiency must therapy, chronic lymphocytic leukemia
be corrected before beginning therapy. and small lymphocytic lymphoma (CLL/
Obtain laboratory baselines, esp. serum SLL) (as monotherapy or in combination
chemistries, renal function. Obtain re- with bendamustine and riTUXimab or with
sults of bone density study. obinutuzumab), CLL/SLL with 17p deletion,
INTERVENTION/EVALUATION
treatment of Waldenstrom’s macroglobulin-
emia (WM) (as monotherapy or in combi-
Monitor electrolytes, esp. serum calcium, nation with rituximab). Marginal zone lym-
phosphate. Monitor renal function tests. phoma (MZL) requiring systemic therapy
PATIENT/FAMILY TEACHING and having received at least one prior anti-
• Expected benefits occur only when CD-20–based therapy. Treatment of chronic
medication is taken with full glass (6–8 graft versus host disease (CGVHD) after fail-
ure of at least one line of systemic therapy. I
oz) of plain water, first thing in the morn-
ing and at least 60 min before first food, PRECAUTIONS
beverage, medication of the day. Any other
Contraindications: Hypersensitivity to
beverage (mineral water, orange juice,
coffee) significantly reduces absorption of ibrutinib. Cautions: Hepatic/renal im-
medication. • Do not chew, crush, dis- pairment, elderly, pregnancy, history of
solve, or divide tablets; swallow GI disease (e.g., bleeding, ulcers).
whole. • Do not lie down for at least 60 ACTION
min after taking medication (potentiates
delivery to stomach, reduces risk of esoph- Inhibits enzymatic activity of Bruton’s tyro-
ageal irritation). • Report swallowing sine kinase (BTK), a signaling molecule that
difficulties, pain when swallowing, chest promotes malignant B-cell proliferation and
pain, new/worsening heartburn. • Con- survival. Therapeutic Effect: Decreases
sider weight-bearing exercises; modify be- malignant B-cell proliferation and survival.
havioral factors (e.g., cigarette smoking, PHARMACOKINETICS
alcohol consumption). • Calcium and
vitamin D supplements should be taken if Readily absorbed following PO. Metabolized
dietary intake inadequate. in liver. Peak plasma concentration: 1–2
hrs. Protein binding: 97%. Excreted in feces
(80%), urine (10%). Half-life: 4–6 hrs.
ibrutinib LIFESPAN CONSIDERATIONS
eye-broo-ti-nib Pregnancy/Lactation: May cause fetal
(Imbruvica) harm. Avoid pregnancy. Unknown if dis-
Do not confuse ibrutinib with tributed in breast milk. Must either discon-
axitinib, dasatinib, erlotinib, tinue drug or discontinue breastfeeding.
gefitinib, imatinib, nilotinib, Children: Safety and efficacy not estab-
PONATinib, SORAfenib, lished. Elderly: Increased risk of cardiac
­SUNItinib, or vandetanib. events (atrial fibrillation, hypertension),
infections (pneumonia, cellulitis), GI
uCLASSIFICATION events (diarrhea, dehydration, bleeding).
PHARMACOTHERAPEUTIC: Bruton
INTERACTIONS
tyrosine kinase inhibitor. CLINICAL:
Antineoplastic. DRUG: Strong CYP3A4 inhibitors (e.g.,
ketoconazole, clarithromycin) may

Canadian trade name Non-Crushable Drug High Alert drug


580 ibrutinib
increase plasma concentration/effect; avoid until resolution to Grade 1 or baseline, then
use. Strong CYP3A4 inducers (e.g., car- reduce dose to 420 mg daily (one capsule
BAMazepine, rifAMPin, phenytoin) may less). If toxicity recurs, interrupt treatment
decrease plasma concentration/effect; avoid until resolution to Grade 1 or baseline, then
use. Anticoagulants (e.g., warfarin), reduce dose to 280 mg once daily (one
antiplatelets (e.g., aspirin, clopido- capsule less). If toxicity still occurs at 280
grel), NSAIDs may increase risk of bleed- mg dose, discontinue treatment.
ing. May decrease the therapeutic effect of
BCG (intravesical), vaccines (live). Concomitant Use of Moderate CYP3A4
May increase adverse/toxic effects of na- Inhibitors (e.g., Fluconazole, DilTIAZem,
talizumab, vaccines (live). HERBAL: St. Verapamil)
John’s wort may decrease concentration/ Start at reduced dose of 140 mg daily. If
effect. FOOD: Grapefruit products, Se- toxicity occurs, either discontinue treat-
ville oranges may increase concentration/ ment or find alternate agent with less
effect. Bitter orange may increase concen- CYP3A inhibition.
I tration/effect. LAB VALUES: May decrease Concomitant Short-Term Use of Strong
Hgb, Hct, neutrophils, platelets. CYP3A4 Inhibitors (7 days or less) (e.g.,
Antifungals, Antibiotics)
AVAILABILITY (Rx)
Interrupt treatment until strong CYP3A
70 mg, 140 mg. Tablets:
Capsules: medications no longer needed.
140 mg, 280 mg, 420 mg, 560 mg.
Concomitant Chronic Use of Strong
ADMINISTRATION/HANDLING CYP3A4 Inhibitors or Inducers
PO Treatment not recommended.
• Give with water. • Swallow capsules/
Dosage in Renal Impairment
tablets whole. Do not break, cut, or open
capsules. Do not break, cut, crush, or divide No dose adjustment.
tablets. Capsules/tablets cannot be chewed. Dosage in Hepatic Impairment
Mild impairment: Decrease dose to
INDICATIONS/ROUTES/DOSAGE 140 mg. Moderate to severe impair-
MCL, MZL ment: Avoid use.
PO: ADULTS, ELDERLY: 560 mg once
daily. Continue until disease progression SIDE EFFECTS
or unacceptable toxicity. Frequent (51%–23%): Diarrhea, fatigue,
musculoskeletal pain, peripheral edema,
CLL/SLL, WM, CGVHD
nausea, bruising, dyspnea, constipation,
PO: ADULTS, ELDERLY: 420 mg once rash, abdominal pain, vomiting. Occa-
daily. Continue until disease progression sional (21%–11%): Decreased appetite,
or unacceptable toxicity. cough, pyrexia, stomatitis, asthenia, dizzi-
Dose Modification ness, muscle spasms, dehydration, head-
Based on Common Terminology Criteria ache, dyspepsia, petechiae, a­ rthralgia.
for Adverse Events (CTCAE). ADVERSE EFFECTS/TOXIC
Any Grade 3 or Greater Nonhematologic REACTIONS
Event, Grade 3 or Greater Neutropenia Anemia, lymphopenia, neutropenia,
with Infection or Fever, or Any Grade 4 thrombocytopenia is expected response
Hematologic Toxicities to therapy. Treatment-emergent myelo-
Interrupt treatment until resolution to suppression (Grade 3–4 CTCAE) re-
Grade 1 or baseline, then restart at initial ported in 41% of pts: neutropenia (29%),
dose. If toxicity recurs, interrupt treatment thrombocytopenia (17%), anemia (9%).

underlined – top prescribed drug


ibuprofen 581
Infections including upper respiratory stools, bruising, nausea, RUQ abdominal
tract infection, UTI, pneumonia, skin in- pain, yellowing of skin or eyes, palpitations,
fection, sinusitis were reported. Hemor- nose bleeds, blood in urine or stool, de-
rhagic events including epistaxis, GI bleed- creased urine output. • Avoid alco-
ing, hematuria, intracranial hemorrhage, hol. • Do not take herbal prod-
subdural hematoma reported in 5% of pts. ucts. • Do not ingest grapefruit
Serious and fatal cases of renal toxicity re- products. • Severe diarrhea may lead to
ported: increased serum creatinine 1.5 dehydration. • Contact physician before
times upper limit of normal (ULN) (67% any planned surgical/dental proce-
of pts), increased serum creatinine 1.53 dures. • Immediately report neurological
times ULN (9% of pts). Second primary changes: confusion, one-sided paralysis,
malignancies including skin cancer (4%), difficulty speaking, partial blindness. • Do
other carcinomas (1%) occurred. not receive live vaccines. • Do not break,
crush, or open capsule.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
I
Obtain baseline vital signs, CBC, serum
chemistries, LFT, PT/INR if on anticoagu-
ibuprofen
lants. Question history of arrhythmias, HF, eye-bue-pro-fen
GI bleed, hepatic/renal impairment, pe- (Advil, Caldolor, Motrin, N­ eoProfen)
ripheral edema, pulmonary disease. Obtain
negative urine pregnancy before initiating j BLACK BOX ALERT jIncreased
risk of serious cardiovascular
treatment. Assess hydration status. Receive thrombotic events, including
full medication history including herbal myocardial infarction, CVA.
products. Assess skin for open/unhealed Contraindicated in setting of CABG
wounds, lesions, moles. Conduct baseline surgery. Increased risk of severe
GI reactions, including ulceration,
neurologic exam. Offer emotional support. bleeding, perforation.
INTERVENTION/EVALUATION Do not confuse Motrin with
Monitor CBC monthly; LFT, serum chem- Neurontin or Advil with Aleve.
istries, renal function routinely. Monitor FIXED-COMBINATION(S)
stool frequency, consistency, character-
istics. Immediately report hemorrhagic Children’s Advil Cold: ibupro-
events: epistaxis, hematuria, hemoptysis, fen/pseudoephedrine (a nasal de-
melena. Encourage PO intake. Obtain congestant): 100 mg/15 mg per 5
ECG for arrhythmias, dyspnea, palpita- mL. Combunox: ibuprofen/oxy-
tions. Screen for possible intracranial CODONE (a narcotic analgesic):
hemorrhage: altered mental status, apha- 400 mg/5 mg. Duexis: ibuprofen/
sia, hemiparesis, unequal pupils, hom- famotidine (an H2 antagonist): 800
onymous hemianopsia (blindness of one mg/26.6 mg. Reprexain CIII:
half of vision on same side of both eyes). ibuprofen/HYDROcodone (a narcotic
Monitor for renal toxicity (anuria, hyper- analgesic): 200 mg/5 mg. Vicopro-
tension, generalized edema, flank pain). fen: ibuprofen/HYDROcodone (a
Assess skin for new lesions. narcotic analgesic): 200 mg/7.5 mg.

PATIENT/FAMILY TEACHING uCLASSIFICATION


• Blood levels will be monitored rou- PHARMACOTHERAPEUTIC: NSAID.
tinely. • Difficulty breathing, fever, cough, CLINICAL: Antirheumatic, analgesic,
burning with urination, body aches, chills antipyretic, antidysmenorrheal, vas-
may indicate acute infection. • Avoid cular headache suppressant.
pregnancy. • Report any black/tarry
Canadian trade name Non-Crushable Drug High Alert drug
582 ibuprofen

USES Rapidly absorbed from GI tract. Protein


Oral: Treatment of fever, inflammatory binding: 90%–99%. Metabolized in liver.
disease, and rheumatoid disorders, osteo- Primarily excreted in urine. Not removed
arthritis, mild to moderate pain, primary by hemodialysis. Half-life: 2–4 hrs.
dysmenorrhea. Caldolor: Mild to moder-
LIFESPAN CONSIDERATIONS
ate pain; severe pain in combination with
an opioid analgesic; fever. NeoProfen: To Pregnancy/Lactation: Unknown if
close a clinically significant patent ductus drug crosses placenta or is distributed
arteriosus (PDA) in premature infants in breast milk. Avoid use during third
weighing between 500 and 1,500 g who are trimester (may adversely affect fetal car-
no more than 32 wks gestational age when diovascular system: premature closure of
usual medical management is ineffective. ductus arteriosus). Children: Safety and
OFF-LABEL: Treatment of cystic fibrosis, efficacy not established in pts younger
pericarditis. Juvenile idiopathic arthritis. than 6 mos. Elderly: GI bleeding, ul-
ceration more likely to cause serious
I PRECAUTIONS adverse effects. Age-related renal impair-
Contraindications: History of hypersensi- ment may increase risk of hepatic/renal
tivity to ibuprofen, aspirin, other NSAIDs. toxicity; reduced dosage recommended.
Treatment of perioperative pain in coronary
INTERACTIONS
artery bypass graft (CABG) surgery. Aspirin
triad (bronchial asthma, aspirin intoler- DRUG: May decrease effects of anti-
ance, rhinitis). NeoProfen: Preterm neo- hypertensives (e.g., amLODIPine,
nates with proven or suspected untreated lisinopril, valsartan), diuretics
infection, elevated total bilirubin, congenital (e.g., furosemide). Aspirin, other
heart disease in whom patency of the patent salicylates may increase risk of GI side
ductus arteriosus is necessary for satisfac- effects, bleeding. May increase effect of
tory pulmonary or systemic blood flow apixaban, dabigatran, edoxaban,
(e.g., pulmonary atresia), bleeding, throm- rivaroxaban, warfarin. Bile acid
bocytopenia, coagulation defects, proven or sequestrants (e.g., cholestyramine)
suspected necrotizing enterocolitis, signifi- may decrease absorption/effect. May in-
cant renal impairment. Cautions: Pts with crease nephrotoxic effect of cycloSPO-
fluid retention, HF, dehydration, coagula- RINE. May increase concentration, risk
tion disorders, concurrent use with aspirin, of toxicity of lithium, methotrexate.
anticoagulants, steroids; history of GI dis- HERBAL: Glucosamine, herbs with
ease (e.g., bleeding, ulcers), smoking, use anticoagulant/antiplatelet proper-
of ­alcohol, elderly, debilitated pts, hepatic/ ties (e.g., garlic, ginger, ginseng,
renal impairment, asthma. ginkgo biloba) may increase con-
centration/effect. FOOD: None known.
ACTION LAB VALUES: May prolong bleeding
Reversibly inhibits COX-1 and COX-2 en- time. May alter serum glucose level. May
zymes, resulting in decreased formation increase serum BUN, creatinine, potas-
of prostaglandin precursors. Thera- sium, ALT, AST. May decrease serum cal-
peutic Effect: Produces analgesic, anti- cium, glucose; Hgb, Hct, platelets.
inflammatory effects; decreases fever.
AVAILABILITY (Rx)
PHARMACOKINETICS Capsules: 200 mg. Injection, Solution:
Route Onset Peak Duration (NeoProfen): 10 mg/mL. (Caldolor): 100
PO (analgesic) 0.5 hr N/A 4–6 hrs
mg/mL. Suspension, Oral: 100 mg/5 mL.
PO 2 days 1–2 N/A Suspension, Oral Drops: 40 mg/mL. Tab-
­(antirheumatic) wks lets: 200 mg, 400 mg, 600 mg, 800 mg.
Tablets, Chewable: 100 mg.

underlined – top prescribed drug


ibuprofen 583

ADMINISTRATION/HANDLING Osteoarthritis, Rheumatoid Disorders


PO: ADULTS, ELDERLY: 400–800 mg 3–4
IV (Caldolor) times/day. Maximum: 3.2 g/day.
Reconstitution • Dilute with D5W or Pain
0.9% NaCl to final concentration of 4 mg/ PO: ADULTS, ELDERLY: 200–400 mg q4–6h
mL or less. prn. Maximum: 3,200 mg/day. CHILDREN
Rate of administration • Infuse over 12 YRS AND OLDER, ADOLESCENTS: 200-400
at least 30 min. mg q4-6h prn. Maximum daily dose:
Storage • Store at room tempera- 1,200 mg/day. CHILDREN 6 MOS–11 YRS: See
ture. • Stable for 24 hrs after dilution. chart under Fever dosing.
IV: ADULTS, ELDERLY: 400–800 mg q6h
IV (Neoprofen) prn. Maximum: 3.2 g/day. CHILDREN,
Reconstitution • Dilute to appro- ADOLESCENTS: (12–17 yrs): 400 mg q4–6h
priate volume with D5W or 0.9% prn. Maximum: 2,400 mg/day. (6 MOS–12
NaCl. • Discard any remaining medica- YRS): 10 mg/kg (maximum dose: 400 I
tion after first withdrawal from vial. mg) q4–6h prn. Maximum: 40 mg/kg/
Rate of administration • Administer day or 2,400 mg, whichever is less.
via IV port nearest the insertion
site. • Infuse continuously over 15 min. Primary Dysmenorrhea
Storage • Store at room tempera- PO: ADULTS: 200–800 mg q4–6h prn.
ture. • Stable for 30 min after dilution. Maximum: 2,400 mg/day.
PO Patent Ductus Arteriosus (PDA)
• Give with food, milk, antacids if GI IV: INFANTS: Initially, 10 mg/kg fol-
distress occurs. lowed by 2 doses of 5 mg/kg at 24 hrs and
48 hrs. All doses based on birth weight.
INDICATIONS/ROUTES/DOSAGE
Fever Dosage in Renal Impairment
PO: ADULTS, ELDERLY: 200–400 mg Hold if anuria or oliguria evident. Avoid
q4–6h prn. CHILDREN 12 YRS AND OLDER, use in severe impairment.
ADOLESCENTS: 200–400 mg q4-6h prn.
Dosage in Hepatic Impairment
Maximum daily dose: 1,200 mg/day.
Avoid use in severe impairment.
CHILDREN 6 MOS AND OLDER:

Weight Dosage SIDE EFFECTS


Occasional (9%–3%): Nausea, vomiting,
kg lbs Age (mg)
dyspepsia, dizziness, rash. Rare (less than
5.4–8.1 12–17 6–11 mos 50 3%): Diarrhea or constipation, flatu-
8.2–10.8 18–23 12–23 mos 75
10.9–16.3 24–35 2–3 yrs 100
lence, abdominal cramps or pain, pruri-
16.4–21.7 36–47 4–5 yrs 150 tus, increased B/P.
21.8–27.2 48–59 6–8 yrs 200
27.3–32.6 60–71 9–10 yrs 250 ADVERSE EFFECTS/TOXIC
32.7–43.2 72–95 11 yrs 300 REACTIONS
Overdose may result in metabolic acidosis.
400 mg q4–6h or
IV: ADULTS, ELDERLY: Rare reactions with long-term use include
100–200 mg q4h prn. Maximum: 3.2 peptic ulcer, GI bleeding, gastritis, severe
g/day. CHILDREN 12–17 YRS: 400 mg hepatic reaction (cholestasis, jaundice),
q4–6h prn. Maximum: 2,400 mg/ nephrotoxicity (dysuria, hematuria, pro-
day. CHILDREN 6 MOS–11 YRS: 10 mg/ teinuria, nephrotic syndrome), severe
kg q4–6h prn. Maximum dose: 400 hypersensitivity reaction (particularly in
mg. Maximum: 40 mg/kg up to 2,400 pts with systemic lupus erythematosus or
mg/day.
Canadian trade name Non-Crushable Drug High Alert drug
584 idelalisib
other collagen diseases). NeoProfen: perforation may occur. Discontinue
Hypoglycemia, hypocalcemia, respiratory if perforation suspected.
failure, UTI, edema, atelectasis may occur.
uCLASSIFICATION
Caldolor: Abdominal pain, anemia, cough,
dizziness, dyspnea, edema, hypertension, PHARMACOTHERAPEUTIC: Phos-
nausea, vomiting have been reported. phatidylinositol 3-kinase inhibitor.
CLINICAL: Antineoplastic.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT USES
Assess onset, type, location, duration of Treatment of relapsed chronic lympho-
pain, inflammation. Inspect appearance of cytic leukemia (CLL), in combination
affected joints for immobility, deformities, with riTUXimab, in pts for whom riTUX-
skin condition. Assess temperature. Ques- imab alone would not be considered
tion medical history as listed in Precautions. appropriate therapy due to other co-­
­
I INTERVENTION/EVALUATION
morbidities. Treatment of relapsed follicu-
lar B-cell non-Hodgkin’s lymphoma (FL)
Monitor for evidence of nausea, dyspep- or relapsed small lymphocytic lymphoma
sia. Assess skin for rash. Observe for (SLL) in pts who have received at least two
bleeding, bruising, occult blood loss. prior systemic therapies.
Evaluate for therapeutic response: relief
of pain, stiffness, swelling; increased joint PRECAUTIONS
mobility; reduced joint tenderness; im- Contraindications: History of serious al-
proved grip strength. Monitor for fever. lergic reactions to idelalisib (e.g., anaphy-
PATIENT/FAMILY TEACHING laxis, toxic epidermal necrolysis). Cautions:
• Avoid aspirin, alcohol during therapy Baseline anemia, leukopenia, neutrope-
(increases risk of GI bleeding). • If GI nia, thrombocytopenia; GI bleeding, he-
upset occurs, take with food, milk, antac- patic impairment. Pts with active infection,
ids. • May cause dizziness. • Report high tumor burden. Avoid concomitant use
ringing in ears, persistent stomach pain, of hepatotoxic or promotility medications.
respiratory difficulty, unusual bruising/ ACTION
bleeding, swelling of extremities, chest
pain/palpitations. Inhibits phosphatidylinositol 3-kinase, which
is highly expressed in malignant lymphoid
B cells. Inhibits several cell-­signaling path-
ways, including B-cell receptor signaling
idelalisib and CXCR4 and CXCR5 signaling, which are
involved in trafficking B cells to lymph nodes
eye-del-a-lis-ib and bone marrow. Therapeutic Effect: In-
(Zydelig) hibits tumor cell growth and metastasis.
j BLACK BOX ALERT jFatal and/ PHARMACOKINETICS
or serious hepatotoxicity may oc-
cur. Monitor LFT prior to and during Well absorbed following PO administra-
treatment. Fatal and/or serious and tion. Metabolized in liver. Protein bind-
severe diarrhea or colitis may oc- ing: 84%. Peak plasma concentration:
cur. Monitor for GI symptoms. Fatal 1.5 hrs. Excreted in feces (78%), urine
and serious pneumonitis may occur.
Monitor for pulmonary symptoms (14%). Half-life: 8.3 hrs.
and bilateral interstitial infiltrates.
Interrupt, then reduce or discon- LIFESPAN CONSIDERATIONS
tinue treatment if hepatotoxicity, Pregnancy/Lactation: May cause fe-
severe diarrhea, or pneumonitis tal harm; avoid pregnancy. Use effective
occurs. Fatal and serious intestinal

underlined – top prescribed drug


idelalisib 585
contraception during treatment and for at than 20 times ULN: Permanently
least 1 mo after discontinuation. Unknown discontinue.
if distributed in breast milk. Must either
discontinue drug or discontinue breast- Elevated Serum Bilirubin
feeding. Children: Safety and efficacy not 1.5–3 times ULN: Monitor serum bili-
established. Elderly: May have increased rubin wkly. Maintain dose. 3–10 times
risk of side effects/adverse reactions. ULN: Monitor serum bilirubin wkly. With-
hold until bilirubin less than 1 times ULN,
INTERACTIONS then resume at 100-mg dose. Greater than
DRUG: Strong CYP3A4 inducers (e.g., 10 times ULN: Permanently discontinue.
carBAMazepine, rifAMPin, phenytoin) Diarrhea
may decrease concentration/effect. Strong Moderate diarrhea: Maintain dose.
CYP3A4 inhibitors (clarithromycin, Severe diarrhea or hospitaliza-
ketoconazole, ritonavir) may increase tion: Withhold until resolved, then re-
concentration/effect. May increase ad- sume at 100-mg dose. Life-threatening
verse effects of natalizumab, vaccines diarrhea: Permanently discontinue.
I
(live). May decrease therapeutic effect
of BCG (intravesical), vaccines (live). Neutropenia
HERBAL: St. John’s wort may decrease ANC 1,000–1,500 cells/mm3: Main-
concentration/effect. Echinacea may tain dose. ANC 500–1,000 cells/
decrease therapeutic effect. FOOD: None mm3: Monitor ANC wkly and main-
known. LAB VALUES: May increase se- tain dose. ANC less than 500 cells/
rum ALT, AST, bilirubin, GGT; triglycerides. mm3: Permanently discontinue.
May decrease Hgb, neutrophils, platelets,
serum sodium. May increase or decrease Thrombocytopenia
lymphocytes, serum glucose. Platelets 50,000–75,000 cells/mm3:
Maintain dose. Platelets 25,000–50,000
AVAILABILITY (Rx) cells/mm3: Monitor platelet count
Tablets: 100 mg, 150 mg. wkly and maintain dose. Platelets less
than 25,000 cells/mm3: Monitor platelet
ADMINISTRATION/HANDLING count wkly. Withhold until platelets greater
PO than 25,000 cells/mm3, then resume at 100-
• Give without regard to food. • Swal- mg dose.
low tablets whole.
Pneumonitis
INDICATIONS/ROUTES/DOSAGE Any symptoms: Permanently discontinue.
Chronic Lymphocytic Leukemia (in
Dosage in Renal Impairment
Combination with RiTUXimab), Follicular
B-cell Non-Hodgkin’s Lymphoma, Small
No dose adjustment.
Lymphocytic Lymphoma Dosage in Hepatic Impairment
PO: ADULTS/ELDERLY: 150 mg twice Use caution. See dose modification.
daily. Continue until disease progression
or unacceptable toxicity. SIDE EFFECTS
Dose Modification CLL
Hepatotoxicity Frequent (35%–21%): Pyrexia, nausea, diar-
Elevated serum ALT, AST 3–5 times rhea, chills. Occasional (10%–5%): Head-
upper limit of normal (ULN): Main- ache, vomiting, generalized pain, arthralgia,
tain dose. 5–20 times ULN: Monitor stomatitis, gastric reflux, nasal congestion.
serum ALT, AST wkly. Withhold until Non-Hodgkin’s Lymphoma
ALT, AST less than 1 times ULN, then Frequent (47%–21%): Diarrhea, fatigue, nau-
resume at 100 mg twice daily. Greater sea, cough, pyrexia, abdominal pain, rash.
Canadian trade name Non-Crushable Drug High Alert drug
586 ifosfamide
Occasional (17%–10%): Dyspnea, decreased failure). Monitor strict I&O, hydration sta-
appetite, vomiting, asthenia, night sweats, in- tus, stool frequency and consistency.
somnia, headache, peripheral edema.
PATIENT/FAMILY TEACHING
ADVERSE EFFECTS/TOXIC • Blood levels will be routinely moni-
REACTIONS tored. Any change in dose or interruption
Thrombocytopenia, neutropenia, leukope- of therapy may require blood draws ev-
nia, lymphopenia are expected responses to ery week. • Avoid pregnancy; do not
therapy, but more severe reactions, includ- breastfeed. • Report abdominal pain,
ing bone marrow failure, febrile neutrope- amber or bloody urine, bruising, black/
nia, may occur. Fatal and/or serious events tarry stools, persistent diarrhea, yellow-
including hepatotoxicity (14% of pts), se- ing of skin or eyes. • Fever, cough,
vere diarrhea or colitis (14% of pts), hyper- burning with urination, body aches,
sensitivity reactions (including anaphylaxis), chills may indicate acute infec-
pneumonitis, intestinal perforation were re- tion. • Avoid alcohol. • Immediately
I ported. Neutropenia occurred in 31% of pts, report difficult breathing, severe cough-
which may greatly increase risk of infection. ing, chest tightness. • Therapy may
Severe skin reactions including toxic epider- cause severe allergic reactions, intestinal
mal necrolysis, generalized rash, exfoliative tearing, or skin rashes or severe diarrhea
rash were reported. Other infections may related to an infected colon. • Do not
include bronchitis, C. difficile colitis, pneu- take any over-the-counter medications
monia, sepsis, UTI. Fatal and/or serious in- including herbal products unless ap-
testinal perforation may occur. proved by your doctor.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT ifosfamide
Obtain ANC, CBC, BMP, LFT, PT/INR, vi-
tal signs, urine pregnancy. Receive full eye-fos-fa-mide
medication history including herbal (Ifex)
products. Question possibility of preg- j BLACK BOX ALERT jHemor-
nancy, current breastfeeding status, use rhagic cystitis may occur. Severe
of contraceptive measures in female pts myelosuppressant. May cause CNS
of reproductive potential. Question his- toxicity, including confusion, coma.
Must be administered by personnel
tory of hypersensitivity reaction or acute trained in administration/handling
skin reactions to drug class. Perform full of chemotherapeutic agents. May
dermatologic exam with routine assess- cause severe nephrotoxicity, result-
ment. Offer emotional support. ing in renal failure.
Do not confuse ifosfamide with
INTERVENTION/EVALUATION cyclophosphamide.
Diligently monitor blood counts (esp.
ANC, CBC, platelet count) frequently. Any uCLASSIFICATION
interruption of therapy or dosage change PHARMACOTHERAPEUTIC: Alkylat-
may require wkly lab monitoring until ing agent. CLINICAL: Antineoplastic.
symptoms resolve. Obtain C. difficile toxin
PCR if severe diarrhea occurs. Screen for
acute cutaneous reactions, allergic reac- USES
tions, other acute infections (sepsis, UTI), Treatment of germ cell testicular carci-
hepatic impairment, pulmonary events noma (used in combination with other
(dyspnea, pneumonitis, pneumonia), or chemotherapy agents and with concurrent
tumor lysis syndrome (electrolyte imbal- mesna for prophylaxis of hemorrhagic
ance, uric acid nephropathy, acute renal cystitis). OFF-LABEL: Small-cell lung,
underlined – top prescribed drug
ifosfamide 587
non–small-cell lung, ovarian, cervical, response to vaccine. HERBAL: Echina-
bladder cancer; soft tissue sarcomas, cea may decrease therapeutic effect.
Hodgkin’s, non-Hodgkin’s lymphomas; FOOD: None known. LAB VALUES: May
osteosarcoma; head and neck, Ewing’s increase serum BUN, bilirubin, creati-
sarcoma. nine, uric acid, ALT, AST.
PRECAUTIONS AVAILABILITY (Rx)
Contraindications: Hypersensitivity to Injection, Powder for Reconstitution: (Ifex):
ifosfamide. Urinary outflow obstruction. 1 g, 3 g. Injection, Solution: 50 mg/mL.
Cautions: Renal/hepatic impairment,
compromised bone marrow reserve, ac- ADMINISTRATION/HANDLING
tive urinary tract infection, preexisting b ALERT c Hemorrhagic cystitis oc-
cardiac disease, prior radiation therapy. curs if mesna is not given concurrently.
Avoid use in pts with WBCs less than Mesna should always be given with ifos-
2,000 cells/mm3 and platelets less than famide.
50,000 cells/mm3. I
IV
ACTION Reconstitution • Reconstitute vial
Inhibits DNA, protein synthesis by cross- with Sterile Water for Injection or Bacte-
linking with DNA strands, preventing cell riostatic Water for Injection to provide
growth. Therapeutic Effect: Produces concentration of 50 mg/mL. Shake to
cellular death (apoptosis). dissolve. • Further dilute with 50–
1,000 mL D5W or 0.9% NaCl to provide
PHARMACOKINETICS concentration of 0.6–20 mg/mL.
Metabolized in liver. Protein binding: Rate of administration • Infuse over
negligible. Crosses blood-brain barrier minimum of 30 min. • Give with at
(to a limited extent). Primarily excreted least 2,000 mL PO or IV fluid (prevents
in urine. Removed by hemodialysis. bladder toxicity). • Give with protec-
Half-life: 11–15 hrs (high dose); 4–7 tant against hemorrhagic cystitis (i.e.,
hrs (low dose). mesna).
Storage • Store vials of powder at
LIFESPAN CONSIDERATIONS room temperature. • Refrigerate vials
Pregnancy/Lactation: If possible, of solution. • After reconstitution with
avoid use during pregnancy, esp. Bacteriostatic Water for Injection, vials
first trimester. Males must use effec- and diluted solutions stable for 24 hrs if
tive contraception and not conceive a refrigerated.
child during treatment and for at least
6 months after discontinuation. May IV INCOMPATIBILITIES
cause fetal harm. Distributed in breast Cefepime (Maxipime), methotrexate.
milk. Breastfeeding not recommended.
Children: Not intended for this pt IV COMPATIBILITIES
population. Elderly: Age-related re- Granisetron (Kytril), ondansetron (Zo-
nal impairment may require dosage fran).
adjustment.
INDICATIONS/ROUTES/DOSAGE
INTERACTIONS b ALERT c Dosage individualized based
DRUG: Bone marrow depressants on clinical response, tolerance to adverse
(e.g., cladribine) may increase myelo- effects. When used in combination therapy,
suppression. Live virus vaccines may consult specific protocols for optimum
potentiate virus r­ eplication, increase vac- dosage, sequence of drug administration.
cine side effects, decrease pt’s antibody

Canadian trade name Non-Crushable Drug High Alert drug


588 iloperidone
Germ Cell Testicular Carcinoma
zations without physician’s approval
IV: ADULTS: 1,200 mg/m2/day for 5 (drug lowers resistance). • Avoid con-
consecutive days. Repeat q3wks or after tact with those who have recently received
recovery from hematologic toxicity. Ad- live virus vaccine. • Avoid crowds, those
minister with mesna and hydration (to with infections. • Report unusual bleed-
prevent bladder toxicity). ing/bruising, fever, chills, sore throat,
Dosage in Renal/Hepatic Impairment joint pain, sores in mouth or on lips, yel-
Use caution. lowing skin or eyes.

SIDE EFFECTS
Frequent (83%–58%): Alopecia, nausea,
vomiting. Occasional (15%–5%): Confu- iloperidone
sion, drowsiness, hallucinations, infection.
Rare (less than 5%): Dizziness, seizures, eye-loe-per-i-doan
disorientation, fever, malaise, stomatitis (Fanapt, Fanapt Titration Pack)
I j BLACK BOX ALERT jElderly pts
(mucosal irritation, glossitis, gingivitis).
with dementia-related psychosis
ADVERSE EFFECTS/TOXIC are at increased risk for mortality
due to cerebrovascular events.
REACTIONS Do not confuse iloperidone with
Hemorrhagic cystitis with hematuria, dysuria amiodarone or dronedarone.
occurs frequently if protective agent (mesna)
is not used. Myelosuppression (leukopenia, uCLASSIFICATION
thrombocytopenia) occurs frequently. Pul- PHARMACOTHERAPEUTIC: Second-
monary toxicity, hepatotoxicity, nephrotoxic- generation (atypical) antipsychotic.
ity, cardiotoxicity, CNS toxicity (confusion, CLINICAL: Antipsychotic.
hallucinations, drowsiness, coma) may re-
quire discontinuation of therapy.
USES
NURSING CONSIDERATIONS Acute treatment of schizophrenia in
adults.
BASELINE ASSESSMENT
Obtain urinalysis before each dose. If PRECAUTIONS
hematuria occurs (greater than 10 RBCs Contraindications: Hypersensitivity to
per field), therapy should be withheld iloperidone. Cautions: Cardiovascular
until resolution occurs. Obtain WBC, disease (HF, history of MI, ischemia, car-
platelet count, Hgb before each dose. Of- diac conduction abnormalities), cerebro-
fer emotional support. vascular disease (increases risk of CVA in
INTERVENTION/EVALUATION pts with dementia, seizure disorders). Pts
at risk for orthostatic hypotension. Pts with
Monitor hematologic studies, urinalysis, bradycardia, hypokalemia, hypomagnese-
renal function, LFT. Assess for fever, sore mia may be at greater risk for torsades
throat, signs of local infection, unusual de pointes. History of seizures, conditions
bruising/bleeding from any site, symp- lowering seizure threshold, high risk of
toms of anemia (excessive fatigue, weak- suicide, risk of aspiration pneumonia,
ness). Monitor for toxicities. congenital QT syndrome, concurrent use
PATIENT/FAMILY TEACHING of medications that prolong QT interval,
• Alopecia is reversible, but new hair decreased GI motility, urinary retention,
growth may have a different color or tex- BPH, xerostomia, visual problems, hepatic
ture. • Drink plenty of fluids (protects impairment, narrow-angle glaucoma, dia-
against cystitis). • Do not have immuni- betes, elderly.

underlined – top prescribed drug


iloperidone 589

ACTION AVAILABILITY (Rx)


Mixed combination of DOPamine type 2 Tablets:1 mg, 2 mg, 4 mg, 6 mg, 8 mg,
(D2) and serotonin type 2 (5-HT2) an- 10 mg, 12 mg.
tagonisms (thought to improve negative
symptoms of psychosis). Therapeutic ADMINISTRATION/
Effect: Diminishes symptoms of schizo- HANDLING
phrenia and reduces incidence of extra- PO
pyramidal side effects. • Give without regard to food. • Tab-
lets may be crushed.
PHARMACOKINETICS
Steady-state concentration occurs in 3–4 INDICATIONS/ROUTES/
days. Well absorbed from GI tract (unaf- DOSAGE
fected by food). Protein binding: 95%. Note: Titrate to the proper dose range
Metabolized in liver. Primarily excreted with dosage adjustments not to exceed 2
in urine, with a lesser amount excreted in mg twice daily (4 mg/day).
feces. Half-life: 18–33 hrs. I
Schizophrenia
LIFESPAN CONSIDERATIONS PO: ADULTS: To avoid orthostatic
Pregnancy/Lactation: Unknown if hypotension, begin with 1 mg twice
drug crosses placenta or is excreted in daily, then adjust dosage to 2 mg
breast milk. Breastfeeding not recom- twice daily, 4 mg twice daily, 6 mg
mended. Children: Safety and efficacy twice daily, 8 mg twice daily, 10 mg
not established. Elderly: More suscep- twice daily, and 12 mg twice daily on
tible to postural hypotension. Increased days 2, 3, 4, 5, 6, and 7, respectively,
risk of cerebrovascular events, mortality, to reach target daily dose of 12–24
including stroke in elderly pts with psy- mg/day in 2 divided doses. Note: Re-
chosis. duce dose by 50% when receiving
strong CYP2D6 or CYP3A4 inhibitors
INTERACTIONS or poor metabolizers of CYP2D6 (see
DRUG: Alcohol, CNS depressants Interactions).
(e.g., diphenhydrAMINE, LORaz- Dosage in Renal Impairment
epam, morphine) may increase CNS No dose adjustment.
depression. Strong CYP3A4 inhibitors
(e.g., clarithromycin, ketoconazole, Dosage in Hepatic Impairment
ritonavir), strong CYP2D6 inhibi- Mild impairment: No adjustment. Mod-
tors (e.g., FLUoxetine, PARoxetine) erate impairment: Use caution. Severe
may increase concentration/effect. Med- impairment: Not recommended.
ications causing prolongation of QT
interval (e.g., amiodarone, dofeti- SIDE EFFECTS
lide, sotalol) may increase effects on Frequent (20%–12%): Dizziness, drowsiness,
cardiac conduction, leading to malig- tachycardia. Occasional (10%–4%): Nau-
nant arrhythmias (torsades de pointes). sea, dry mouth, nasal congestion, weight
HERBAL: Herbals with sedative prop- increase, diarrhea, fatigue, orthostatic
erties (e.g., chamomile, kava kava, hypotension. Rare (3%–1%): Arthralgia,
valerian) may increase CNS depression. musculoskeletal stiffness, abdominal
FOOD: None known. LAB VALUES: May discomfort, nasopharyngitis, tremor,
increase serum prolactin levels. hypotension, rash, ejaculatory failure,
­
dyspnea, blurred vision, lethargy.

Canadian trade name Non-Crushable Drug High Alert drug


590 imatinib

ADVERSE EFFECTS/TOXIC
REACTIONS imatinib
Extrapyramidal disorders, including tar-
im-at-in-ib
dive dyskinesia (protrusion of tongue,
(Gleevec)
puffing of cheeks, chewing/puckering of
Do not confuse imatinib with
the mouth), occur in 4% of pts. Upper
dasatinib, erlotinib, lapat-
respiratory infection occurs in 3% of pts.
inib, nilotinib, SORAfenib, or
QT interval prolongation may produce
SUNItinib.
torsades de pointes, a form of ventricular
tachycardia. Neuroleptic malignant syn- uCLASSIFICATION
drome (e.g., hyperpyrexia, muscle rigid-
PHARMACOTHERAPEUTIC: BCR-ABL
ity, altered mental status, irregular pulse
tyrosine kinase inhibitor. CLINI-
or B/P) has been noted.
CAL: Antineoplastic.
NURSING CONSIDERATIONS
I
BASELINE ASSESSMENT USES
Assess pt’s behavior, appearance, emo- Newly diagnosed chronic-phase Phila-
tional status, response to environment, delphia chromosome positive chronic
speech pattern, thought content. ECG myeloid leukemia (Ph+ CML) in chil-
should be obtained to assess for QT dren and adults. Pts in blast crisis, ac-
prolongation before instituting medica- celerated phase, or chronic phase Ph+
tion. Question medical history as listed in CML who have already failed interferon
Precautions. therapy. Adults with relapsed or refrac-
INTERVENTION/EVALUATION tory Ph+ acute lymphoblastic leukemia
(ALL). Treatment in children with Ph+
Monitor for orthostatic hypotension; as- ALL. Adults with myelodysplastic/myelo-
sist with ambulation. Monitor for fine proliferative disease (MDS/MPD) associ-
tongue movement (may be first sign of ated with platelet-derived growth factor
tardive dyskinesia, possibly irreversible). receptor (PDGFR) gene rearrangements.
Monitor serum potassium, magnesium in Adults with aggressive systemic mastocyto-
pts at risk for electrolyte disturbances. sis (ASM) without mutation of the D816V
Assess for therapeutic response (greater c-Kit or unknown mutation status of the
interest in surroundings, improved self- c-Kit. Adults with hypereosinophilic syn-
care, increased ability to concentrate, drome (HES) and/or chronic eosinophilic
relaxed facial expression). leukemia (CEL) with positive, negative, or
PATIENT/FAMILY TEACHING unknown FIP1L1-PDGFR fusion kinase.
• Avoid tasks that require alertness, Adults with dermatofibrosarcoma protu-
­motor skills until response to drug is es- berans (DFSP) that is unresectable, recur-
tablished. • Be alert to symptoms of rent, and/or metastatic. Pts with malignant
orthostatic hypotension; slowly go from gastrointestinal stromal tumors (GIST)
lying to standing. • Report if feeling that are unresectable and/or metastatic.
faint, if experiencing heart palpitations, Prevention of cancer recurrence in pts
or if fever or muscle rigidity occurs. following surgical removal of GIST. OFF-
• Report extrapyramidal symptoms LABEL: Treatment of desmoid tumors (soft
(e.g., involuntary muscle movements, tissue sarcoma). Post–stem cell transplant
tics) immediately. (allogeneic), follow-up treatment in re-
current CML. Treatment of advanced or
metastatic melanoma.

underlined – top prescribed drug


imatinib 591

PRECAUTIONS AVAILABILITY (Rx)


Contraindications: Hypersensitivity to ima­ Tablets: 100 mg, 400 mg.
tinib. Cautions: Hepatic/renal impairment,
thyroidectomy pts, hypothyroidism, gastric ADMINISTRATION/HANDLING
surgery pts. Pts in whom fluid accumula- PO
tion is poorly tolerated (e.g., HF, hyperten- • Give with a meal and large glass of
sion, pulmonary d­ isease). water. • Tablets may be dispersed in
water or apple juice (stir until dissolved;
ACTION give immediately). Do not crush or chew
Inhibits Bcr-Abl tyrosine kinase, an tablets.
enzyme created by Philadelphia chro-
mosome abnormality found in pts with INDICATIONS/ROUTES/DOSAGE
chronic myeloid leukemia. Therapeutic Ph+ Chronic Myeloid Leukemia (CML)
Effect: Blocks tumor cell proliferation (Chronic Phase)
and induces cellular death (apoptosis). PO: ADULTS, ELDERLY: 400 mg once
I
daily; may increase to 600 mg/day. Maxi-
PHARMACOKINETICS mum: 800 mg. CHILDREN: 340 mg/m2/
Well absorbed after PO administration. day. Maximum: 600 mg.
Protein binding: 95%. Metabolized in liver.
Eliminated in feces (68%), urine (13%). Ph+ CML (Accelerated Phase)
Half-life: 18 hrs; metabolite, 40 hrs. PO: ADULTS, ELDERLY: 600 mg once daily.
May increase to 800 mg/day in 2 divided
LIFESPAN CONSIDERATIONS doses (400 mg twice daily). CHILDREN:
Pregnancy/Lactation: May cause fetal 340 mg/m2/day. Maximum: 600 mg.
harm. Breastfeeding not recommended.
Children: Safety and efficacy not estab- Ph+ Acute Lymphoblastic Leukemia (ALL)
lished. Elderly: Increased frequency of PO: ADULTS, ELDERLY: 600 mg once
fluid retention. daily.
INTERACTIONS Gastrointestinal Stromal Tumors (GIST)
DRUG: CYP3A4 inducers (e.g., carBA- (Following Complete Resection)
Mazepine, phenytoin, rifAMPin) may PO: ADULTS, ELDERLY: 400 mg once
decrease concentration/effect. CYP3A4 daily for 3 yrs.
inhibitors (e.g., clarithromycin, ke-
GIST (Unresectable)
toconazole, ritonavir) may increase
concentration/effect. Bone marrow PO: ADULTS, ELDERLY: 400 mg once daily.
depressants (e.g., cladribine) may May increase up to 400 mg twice daily.
increase myelosuppression. Live virus Aggressive Systemic Mastocytosis (ASM)
vaccines may potentiate virus replication, with Eosinophilia
increase vaccine side effects, decrease pt’s PO: ADULTS, ELDERLY: Initially, 100 mg/
antibody response to vaccine. May de- day. May increase up to 400 mg/day.
crease effect of warfarin. HERBAL: Echi-
nacea may decrease therapeutic effect. ASM Without Mutation of the D816V C-Kit
St. John’s wort decreases concentration. or Unknown Mutation Status of C-Kit
FOOD: Grapefruit products may increase PO: ADULTS, ELDERLY: 400 mg once
concentration. LAB VALUES: May increase daily.
serum bilirubin, ALT, AST, creatinine. May
decrease platelet count, RBC, WBC count; Dermatofibrosarcoma Protuberans (DFSP)
serum potassium, albumin, calcium. PO: ADULTS, ELDERLY: 400 mg twice
daily.

Canadian trade name Non-Crushable Drug High Alert drug


592 imatinib
Hypereosinophilic Syndrome (HES)/ somnolence. Rare (less than 10%): Naso-
Chronic Eosinophilic Leukemia (CEL) pharyngitis, petechiae, asthenia, epistaxis.
PO: ADULTS, ELDERLY: 400 mg once
daily. ADVERSE EFFECTS/TOXIC
REACTIONS
HES/CEL with Positive or Unknown Severe fluid retention (pleural effusion,
FIP1L1-PDGFR Fusion Kinase pericardial effusion, pulmonary edema,
PO: ADULTS, ELDERLY: Initially, 100 mg/ ascites), hepatotoxicity occur rarely.
day. May increase up to 400 mg/day. Neutropenia, thrombocytopenia are ex-
Myelodysplastic/Myeloproliferative
pected responses to the therapy. Respi-
Disease (MDS/MPD)
ratory toxicity is manifested as dyspnea,
PO: ADULTS, ELDERLY: 400 mg once pneumonia. Heart damage (left ventricu-
daily. lar dysfunction, HF) may occur.

Usual Dosage for Children (2 Yrs and NURSING CONSIDERATIONS


I Older) BASELINE ASSESSMENT
Ph+ CML (Chronic Phase, Recurrent, or
Obtain baseline CBC, serum chemistries,
Resistant)
renal function test. Monitor LFT before
PO: 340 mg/m2/day. Maximum: 600
beginning treatment, monthly thereaf-
mg/day. ter. Offer emotional support.
Ph+ CML (Chronic Phase, Newly
Diagnosed, Ph+ ALL) INTERVENTION/EVALUATION
PO: 340 mg/m2/day. Maximum: 600 Assess periorbital area, lower extremi-
mg/day. ties for early evidence of fluid retention.
Dosage with Strong CYP3A4 Inducers
Monitor for unexpected, rapid weight
Increase dose by 50% with careful moni- gain. Offer antiemetics to control nau-
toring. sea, vomiting. Monitor daily pattern of
bowel activity, stool consistency. Moni-
Dosage in Renal Impairment tor CBC wkly for first mo, biweekly for
second mo, periodically thereafter for
Creatinine evidence of neutropenia, thrombocyto-
Clearance Maximum Dose penia; assess hepatic function tests for
40–59 mL/min 600 mg hepatotoxicity. Monitor renal function,
20–39 mL/min 400 mg serum electrolytes. Duration of neutro-
Less than 20 mL/min 100 mg penia or thrombocytopenia ranges from
2–4 wks.
Dosage in Hepatic Impairment
Mild to moderate impairment: No PATIENT/FAMILY TEACHING
adjustment. Severe impairment: Re- • Avoid crowds, those with known infec-
duce dosage by 25%. tion. • Avoid contact with anyone who
recently received live virus vaccine; do
SIDE EFFECTS not receive vaccinations. • Take with
Frequent (68%–24%): Nausea, diarrhea, food and a full glass of water. • Avoid
vomiting, headache, fluid retention, rash, grapefruit products. • Report chest
musculoskeletal pain, muscle cramps, ar- pain, swelling of extremities, weight gain
thralgia. Occasional (23%–10%): Abdomi- greater than 5 lb, easy bruising/bleeding.
nal pain, cough, myalgia, fatigue, fever, • Avoid tasks that require alertness,
anorexia, dyspepsia, constipation, night ­motor skills until response to drug is
sweats, pruritus, dizziness, blurred vision, ­established.

underlined – top prescribed drug


immune globulin IV 593
ciency, hyperprolinemia (Hizentra,
immune globulin Privigen), severe thrombocytopenia,
coagulation disorders where IM injec-
IV (IGIV) tions contraindicated. Hypersensitivity
to corn (Octagam); infants/neonates
im-mune glob-u-lin for whom sucrose or fructose toler-
(Bivigam, Carimune NF, Flebogamma ance has not been established (Gam-
DIF, Gammagard Liquid, Gamma- maplex). Cautions: Cardiovascular
gard S/D, Gammaplex, Gamunex-C, disease, history of thrombosis, renal
Hizentra, Octagam 5%, Privigen) impairment.
j BLACK BOX ALERT jAcute
renal impairment characterized by ACTION
increased serum creatinine, oliguria,
acute renal failure, osmotic nephro- Replacement therapy for primary/
sis, particularly pts with any degree secondary immunodeficiencies and
of renal insufficiency, diabetes mel- lgG antibodies against bacteria, viral
litus, volume depletion, sepsis, and antigens; interferes with receptors on I
those older than age 65 yrs. Throm- cells of reticuloendothelial system for
bosis may occur (administer at the
minimum dose and minimum infusion autoimmune cytopenias/idiopathic
rate; ensure adequate hydration). thrombocytopenia purpura (ITP); in-
creases antibody titer and antigen-anti-
uCLASSIFICATION body reaction potential. Therapeutic
PHARMACOTHERAPEUTIC: Immune Effect: Provides passive immunity
globulin, blood product. CLINI- replacement for immunodeficiencies,
CAL: Immunizing agent. increases antibody titer.
PHARMACOKINETICS
USES Evenly distributed between intravascular
Treatment of pts with primary humoral and extravascular space. Half-life: 21–
immunodeficiency syndromes, acute/ 23 days.
chronic immune idiopathic thrombo-
cytopenic purpura (ITP), prevention LIFESPAN CONSIDERATIONS
of coronary artery aneurysms associ- Pregnancy/Lactation: Unknown if
ated with Kawasaki disease, prevention drug crosses placenta or is distributed in
of recurrent bacterial infections in pts breast milk. Children/Elderly: No age-
with hypogammaglobulinemia associ- related precautions noted.
ated with B-cell chronic lymphocytic
leukemia (CLL). Treatment of chronic INTERACTIONS
inflammatory demyelinating polyneu- DRUG: Live virus vaccines may in-
ropathies. Provide passive immunity in crease vaccine side effects, potentiate
pts with hepatitis A, measles, rubella, virus replication, decrease pt’s antibody
varicella. OFF-LABEL: Guillain-Barré syn- response to vaccine. HERBAL: None sig-
drome; myasthenia gravis; prevention of nificant. FOOD: None known. LAB VAL-
acute infections in immunosuppressed UES: None significant.
pts; prevention, treatment of infection
in high-risk, preterm, low-birth-weight AVAILABILITY (Rx)
neonates; treatment of multiple sclerosis, Injection, Powder for Reconstitution: (Cari-
HIV-associated thrombocytopenia. mune NF): 3 g, 6 g, 12 g. (Gammagard
S/D): 5 g, 10 g. Injection, Solution: (Bivigam
PRECAUTIONS 10%, Flebogamma DIF 5%, 10%, Gammagard
Hypersensitivity to
Contraindications: Liquid 10%, Gammaplex 5%, Gamunex-C
immune globulin. Selective IgA defi- 10%, Octagam 5%, Privigen 10%).

Canadian trade name Non-Crushable Drug High Alert drug


594 immune globulin IV (IGIV)

ADMINISTRATION/HANDLING for 4 consecutive days. Begin within 7 days


IV of onset of fever. American Heart Asso-
ciation guidelines: 2,000 mg/kg as a
b ALERT c Monitor vital signs, B/P dili- single dose given over 10–12 hrs within
gently during and immediately after IV 10 days of disease onset.
administration (precipitous fall in B/P
may indicate anaphylactic reaction). Stop Chronic Lymphocytic Leukemia (CLL)
infusion immediately. EPINEPHrine IV: ADULTS, ELDERLY, CHILDREN: (Gam-
should be readily available. magard): 400 mg/kg/dose q3–4wks.
Reconstitution • Reconstitute only
Chronic Inflammatory Demyelinating
with diluent provided by manufac-
Polyneuropathy
turer. • Discard partially used or turbid
IV: ADULTS, ELDERLY, CHILDREN: (Gam­
preparations.
unex-C): Loading Dose: 2 g/kg divided
Rate of administration • Give by in-
fusion only. • After reconstitution, ad- over 2–4 days (consecutive). Mainte-
I minister via separate tubing. • Rate of nance: 1 g/kg/day q3wks or 500 mg/
infusion varies with product used. kg for 2 consecutive days q3wks. (Privi-
gen): Loading Dose: 2 g/kg in divided
Storage • Refer to individual IV prep-
arations for storage requirements, stabil- doses over 2-5 consecutive days. Mainte-
ity after reconstitution. nance: 1 g/kg q3wks or 500 mg/kg for 2
consecutive days q3wks.
IV INCOMPATIBILITIES
Dosage in Renal Impairment
Do not mix with any other medications. Caution when giving IV.
INDICATIONS/ROUTES/DOSAGE Dosage in Hepatic Impairment
Primary Immunodeficiency Syndrome No dose adjustment.
IV: ADULTS, ELDERLY, CHILDREN: (Privi-
gen): 200–800 mg/kg q3–4wks. (Cari- SIDE EFFECTS
mune NF): 400–800 mg/kg q3–4 wks. Frequent: Tachycardia, backache, head-
(Flebogamma DIF, Gammagard, ache, arthralgia, myalgia. Occasional: Fa-
Gamunex-C, Octagam): 300–600 mg/ tigue, wheezing, injection site rash/pain,
kg/q3–4wks. (Bivigam, Gammaplex): leg cramps, urticaria, bluish color of lips/
300–800 mg/kg q3–4wks. nailbeds, light-headedness.
Idiopathic Thrombocytopenic ADVERSE EFFECTS/TOXIC
Purpura (ITP) REACTIONS
IV: ADULTS, ELDERLY, CHILDREN: (Cari- Anaphylactic reactions occur rarely, but
mune NF): 400 mg/kg/day for 2–5 days. incidence increases with repeated injec-
Maintenance: 400–1,000 mg/kg/dose tions. EPINEPHrine should be readily
to maintain platelet count or control available. Overdose may produce chest
bleeding. (Gammagard): 1,000 mg/kg: tightness, chills, diaphoresis, dizziness,
up to 3 total doses may be given on al- facial flushing, nausea, vomiting, fever, hy-
ternate days based on pt response and/ potension. Hypersensitivity reaction (anxi-
or platelet count. (Gammaplex, Octa- ety, arthralgia, dizziness, flushing, myalgia,
gam, Flebogamma DIF): 1,000 mg/kg palpitations, pruritus) occurs rarely.
once daily for 2 consecutive days.
NURSING CONSIDERATIONS
Kawasaki Disease
Note: Must be used with aspirin. BASELINE ASSESSMENT
IV: CHILDREN: (Gammagard): 1,000 Inquire about exposure history to dis-
mg/kg as single dose or 400 mg/kg/day ease for pt/family as appropriate. Have

underlined – top prescribed drug


indacaterol/­glycopyrrolate 595
EPINEPHrine readily available. Pt should Contraindications:Hypersensitivity to
be well hydrated prior to administration. indacaterol. Monotherapy in treatment
of asthma. Cautions: Cardiovascular
INTERVENTION/EVALUATION disease (coronary insufficiency, arrhyth-
Control rate of IV infusion carefully; too- mias, hypertension, history of hypersen-
rapid infusion increases risk of precipi- sitivity to sympathomimetics), seizure
tous fall in B/P, signs of anaphylaxis (­ facial disorders, hyperthyroidism, hypokale-
flushing, chest tightness, chills, fever, mia, diabetes. May cause paradoxical
nausea, vomiting, diaphoresis). Assess bronchospasm, severe asthma.
pt closely during infusion, esp. first hr;
monitor vital signs continuously. Stop in- ACTION
fusion if aforementioned signs noted. For Indacaterol: Stimulates beta2-adrenergic
treatment of idiopathic thrombocytopenic receptors in lungs, resulting in relaxation
purpura (ITP), monitor platelet count. of bronchial smooth muscle. Glycopyr-
PATIENT/FAMILY TEACHING
rolate: Inhibits action of acetylcholine at
muscarinic receptor. Therapeutic Ef- I
• Explain rationale for therapy. • Re- fect: Relieves bronchospasm, reduces air-
port sudden weight gain, fluid retention, way resistance, improves bronchodilation.
edema, decreased urine output, short-
ness of breath. PHARMACOKINETICS
Extensive activation of systemic beta-
adrenergic receptors; acts primarily
in lungs. Protein binding: 94%–95%.
indacaterol/­ Metabolized in liver. Steady-state level:
glycopyrrolate 12–15 days. Primarily excreted in feces.
Half-life: 45–126 hrs.
in-da-ka-ter-ol/glye-koe-pir-oh-late LIFESPAN CONSIDERATIONS
(Utibron Neohaler, Ultibro
Breezhaler ) Pregnancy/Lactation: Unknown if
drug crosses placenta or is distributed in
j BLACK BOX ALERT j Long- breast milk. Children: Safety and efficacy
acting beta2-adrenergic agonists
(LABAs) have an increased risk of not established. Elderly: May be more
asthma-related deaths. Not indi- sensitive to tremor, tachycardia due to age-
cated for treatment of asthma. related increased sympathetic sensitivity.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Beta2- INTERACTIONS
adrenergic agonist, anticholinergic. DRUG: Aclidinium, ipratropium,
CLINICAL: Bronchodilator. tiotropium, umeclidinium may in-
crease anticholinergic effect. Beta
blockers (e.g., atenolol, carvedilol,
USES metoprolol) may decrease therapeutic
Long-term maintenance treatment of effect. May increase concentration/effects
airflow obstruction in pts with chronic of corticosteroids (e.g., dexametha-
obstructive pulmonary disease (COPD), sone, predniSONE), loop diuretics
including chronic bronchitis and emphy- (e.g., bumetanide, furosemide),
sema. thiazide/thiazide-like diuretics
(e.g., hydroCHLOROthiazide). QT
PRECAUTIONS interval–­ prolonging drugs (e.g.,
b ALERT c Not indicated for the treat- amiodarone, ciprofloxacin, haloper-
ment of asthma, acute exacerbations of idol), MAOIs (e.g., phenelzine, sele-
COPD. giline) may increase concentration/effect.

Canadian trade name Non-Crushable Drug High Alert drug


596 indacaterol/­glycopyrrolate
HERBAL: None significant. FOOD: None ADVERSE EFFECTS/TOXIC
known. LAB VALUES: May decrease REACTIONS
serum potassium. May increase serum Peripheral edema, diabetes mellitus,
glucose. hyperglycemia, sinusitis, URI reported
AVAILABILITY (Rx) in greater than 2% of pts. Excessive sym-
pathomimetic stimulation, hypokalemia
Capsule for Inhalation:(indacaterol/gly- may produce palpitations, arrhythmias,
copyrrolate) 27.5 mcg/15.6 mcg. angina pectoris, tachycardia, muscle
ADMINISTRATION/ cramps, weakness. Hyperglycemia symp-
HANDLING toms present with increased thirst, poly-
uria, dry mouth, drowsiness/confusion,
Inhalation
blurred vision. Severe shortness of breath
• Do not shake or prime. • Open cap
may indicate paradoxical bronchospasm,
of Neohaler by pulling upward, then
deteriorating COPD. Serious asthma-
open mouthpiece. • Remove capsule
related events, including death, reported.
I from blister package and place in center
of chamber. Firmly close until click is NURSING CONSIDERATIONS
heard. • Hold inhaler upright and
pierce capsule by pressing side buttons BASELINE ASSESSMENT
once only. • Instruct pt to exhale com- Assess rate, depth, rhythm, type of respi-
pletely. Place mouthpiece into mouth, rations. Monitor ECG, serum potassium,
close lips, and inhale quickly and deeply ABG determinations, O2 saturation, pul-
through mouth (this causes capsule to monary function test. Assess lung sounds
spin, dispensing the drug). A slight whir- for wheezing (bronchoconstriction),
ring noise should occur. If not, this may rales. Obtain baseline electrolytes, blood
indicate capsule is stuck. Gently tap in- glucose. Receive full medication history
haler to loosen and reattempt. • Pt and screen for possible drug interactions.
should hold breath as long as possible Question for history of asthma, angina
before exhaling. • Check capsule to en- pectoris, diabetes, peripheral edema.
sure that all the powder is gone. Instruct
pt to reinhale if powder remains. INTERVENTION/EVALUATION
Storage • Store at room tempera- Routinely monitor serum electrolytes, blood
ture. • Maintain capsules within indi- glucose, O2 saturation. Recommend dis-
vidual blister pack until time of continuation of short-acting beta2-agonists
use. • Do not store capsules in Neo- (use only for symptomatic relief of acute
haler device. respiratory symptoms). Monitor for palpi-
tations, tachycardia, serum hypokalemia.
INDICATIONS/ROUTES/ Inspect oropharyngeal cavity for irritation.
DOSAGE
PATIENT/FAMILY TEACHING
Maintenance Therapy and Prevention of
COPD • Follow manufacturer guidelines for
Inhalation: ADULTS, ELDERLY: 1 capsule proper use of inhaler. • Increase fluid
inhaled twice daily. intake (decreases lung secretion viscos-
ity). • Rinse mouth with water after in-
Dosage in Renal/Hepatic Impairment halation to decrease mouth/throat irrita-
No dose adjustment. tion. • Avoid excessive use of caffeine
derivatives (chocolate, coffee, tea,
SIDE EFFECTS cola). • An immediate cough lasting 15
Occasional (7%–5%): Cough, nasophar- sec may occur after inhaler use. • Re-
yngitis, headache. Rare (2%): Oropha- port any fever, productive cough, body
ryngeal pain, nausea. aches, difficulty breathing.

underlined – top prescribed drug


indapamide 597

INTERACTIONS
indapamide DRUG: May increase risk of lithium
toxicity. Bile acid sequestrants (e.g.,
in-dap-a-mide
cholestyramine) may decrease absorp-
(Lozide )
tion/effect. May increase QT interval–­
Do not confuse indapamide with
prolonging effect of dofetilide. May
Iopidine.
increase the hypokalemic effect of topi-
uCLASSIFICATION ramate. HERBAL: Licorice may increase
the hypokalemic effect. Herbals with
PHARMACOTHERAPEUTIC: Thiazide.
hypotensive properties (e.g., garlic,
CLINICAL: Diuretic, antihypertensive.
ginger, ginkgo biloba) or hyperten-
sive properties (e.g., yohimbe) may
USES alter effect. FOOD: None known. LAB
VALUES: May increase uric acid, plasma
Management of mild to moderate hyperten-
sion. Treatment of edema associated with renin activity. May decrease protein-
HF. OFF-LABEL: Calcium nephrolithiasis. bound iodine; serum calcium, potas- I
sium, sodium.
PRECAUTIONS AVAILABILITY (Rx)
Contraindications: Hypersensitivity to in- Tablets: 1.25 mg, 2.5 mg.
dapamide. Anuria, sulfonamide-derived
drugs. Cautions: History of hypersen- ADMINISTRATION/
sitivity to sulfonamides or thiazide di- HANDLING
uretics. Severe renal disease, hepatic PO
impairment, history of gout, prediabetes, • Give with food, milk if GI upset oc-
diabetes, elderly, severe hyponatremia, curs, preferably with breakfast (may pre-
elevated serum cholesterol. vent nocturia).
ACTION INDICATIONS/ROUTES/
Diuretic: Blocks reabsorption of wa- DOSAGE
ter, sodium, potassium at cortical di- Edema
luting segment of distal renal tubule. PO: ADULTS: Initially, 2.5 mg/day, may
Antihypertensive: Reduces plasma, increase to 5 mg/day after 1 wk.
­extracellular fluid volume, and periph-
eral vascular resistance by direct effect Hypertension
on blood vessels. Therapeutic Ef- PO: ADULTS, ELDERLY: Initially, 1.25 mg.
fect: Promotes diuresis, reduces B/P. May increase to 2.5 mg/day after 4 wks
or 5 mg/day after additional 4 wks. Usual
PHARMACOKINETICS dose: 1.25–2.5 mg/day.
Almost completely absorbed follow-
ing PO administration. Protein binding: Dosage in Renal/Hepatic Impairment
71%–79%. Metabolized in liver. Excreted Use caution.
in urine. Half-life: 14–18 hrs.
SIDE EFFECTS
LIFESPAN CONSIDERATIONS Frequent (5% and greater): Fatigue, par-
Pregnancy/Lactation: Unknown if esthesia of extremities, tension, irritabil-
drug crosses placenta or is distributed ity, agitation, headache, dizziness, light-
in breast milk. Children: Safety and ef- headedness, insomnia, muscle cramps.
ficacy not established. Elderly: May be Occasional (less than 5%): Urinary
more sensitive to hypotensive, electrolyte frequency, urticaria, rhinorrhea, flush-
effects. ing, weight loss, orthostatic h­ ypotension,

Canadian trade name Non-Crushable Drug High Alert drug


598 indomethacin
depression, blurred vision, nausea,
vomiting, diarrhea, constipation, dry indomethacin
mouth, impotence, rash, pruritus.
in-doe-meth-a-sin
ADVERSE EFFECTS/TOXIC (Indocin, Tivorbex)
REACTIONS j BLACK BOX ALERT jIncreased
Vigorous diuresis may lead to profound risk of serious cardiovascular
thrombotic events, including
water and electrolyte depletion, resulting myocardial infarction, CVA. In-
in hypokalemia, hyponatremia, dehydra- creased risk of severe GI reactions,
tion. Acute hypotensive episodes may oc- including ulceration, bleeding,
cur. Hyperglycemia may be noted during perforation.
prolonged therapy. Pancreatitis, blood Do not confuse Indocin with
dyscrasias, pulmonary edema, allergic Imodium, Minocin, or Vicodin.
pneumonitis, dermatologic reactions oc-
uCLASSIFICATION
cur rarely. Overdose can lead to lethargy,
I coma without changes in electrolytes or PHARMACOTHERAPEUTIC: NSAID.
hydration. CLINICAL: Anti-inflammatory, anal-
gesic.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT USES
Obtain vital signs, esp. B/P for hypo- Indocin: Treatment of active stages of
tension, before administration. Assess rheumatoid arthritis, osteoarthritis, an-
baseline electrolytes, particularly hypo- kylosing spondylitis, acute gouty arthri-
kalemia. Observe for edema; assess skin tis. Relieves acute bursitis, tendinitis.
turgor, mucous membranes for hydration Tivorbex: Treatment of mild to moder-
status. Assess muscle strength, mental ate acute pain in adults. IV: For closure
status. Note skin temperature, moisture. of hemodynamically significant patent
Obtain baseline weight. ductus arteriosus of premature infants
INTERVENTION/EVALUATION weighing between 500 and 1,750 g when
48-hr usual medical management is inef-
Continue to monitor B/P, vital signs,
fective. OFF-LABEL: Management of pre-
electrolytes, I&O, weight. Note extent
term labor.
of diuresis. Watch for electrolyte dis-
turbances (hypokalemia may result PRECAUTIONS
in weakness, tremor, muscle cramps,
Contraindications: Hypersensitivity to as-
nausea, vomiting, altered mental sta-
pirin, indomethacin, other NSAIDs. Peri-
tus, tachycardia; hyponatremia may re-
operative pain in setting of CABG surgery.
sult in confusion, thirst, cold/clammy
History of asthma, urticaria, allergic reac-
skin).
tions after taking aspirin, other NSAIDs.
PATIENT/FAMILY TEACHING Suppositories: History of proctitis,
• Expect increased frequency, volume of recent rectal bleeding. ­Injection: In
urination (diminishes with long-term preterm infants with untreated/systemic
use). • To reduce hypotensive effect, infection or congenital heart disease
go slowly from lying to standing. • Eat where patency of PDA necessary for pul-
foods high in potassium such as whole monary or systemic blood flow; bleeding,
grains (cereals), legumes, meat, ba- thrombocytopenia, coagulation defects,
nanas, apricots, orange juice, potatoes necrotizing enterocolitis, significant re-
(white, sweet), raisins. • Take early in nal dysfunction. Cautions: Cardiac dys-
the day to avoid nocturia. function, fluid retention, HF, hyperten-
sion, renal/hepatic impairment, epilepsy;

underlined – top prescribed drug


indomethacin 599
concurrent aspirin, steroids, anticoagu- May increase serum BUN, creatinine, po-
lant therapy. Treatment of juvenile rheu- tassium, ALT, AST. May decrease serum
matoid arthritis in children. History of sodium, platelet count, leukocytes.
GI disease (bleeding or ulcers), elderly,
debilitated, asthma, depression, Parkin- AVAILABILITY (Rx)
son’s disease. Capsules: 25 mg, 50 mg. (Tivorbex): 20
mg, 40 mg. Injection, Powder for Recon-
ACTION stitution: (Indocin IV): 1 mg. Oral Suspen-
Reversibly inhibits COX-1 and COX-2 en- sion: (Indocin): 25 mg/5 mL. Supposi-
zymes. Produces antipyretic, analgesic, tory: 50 mg.
anti-inflammatory effects by inhibiting
prostaglandin synthesis. Therapeutic Capsules, Extended-Release: 75 mg.
Effect: Reduces inflammatory response, ADMINISTRATION/HANDLING
fever, intensity of pain. Closure of patent
ductus arteriosus. IV
I
PHARMACOKINETICS Reconstitution • To 1-mg vial, add
1–2 mL preservative-free Sterile Water
Route Onset Peak Duration for Injection or 0.9% NaCl to provide
PO 30 min — 4–6 hrs concentration of 1 mg/mL or 0.5 mg/mL,
Well absorbed from GI tract. Protein respectively. • Do not further dilute.
Rate of administration • Administer
binding: 99%. Metabolized in liver. Ex-
creted in urine. Half-life: 4.5 hrs. over 20–30 min.
Storage • Use IV solution immediately
LIFESPAN CONSIDERATIONS following reconstitution. • IV solution
Pregnancy/Lactation: Crosses pla- appears clear; discard if cloudy or
centa; distributed in breast milk. Avoid precipitate forms. • Discard unused
use during third trimester. Chil- portion.
dren: Safety and efficacy not estab- PO
lished in those younger than 14 yrs. El- • Give after meals or with food, antac-
derly: Increased risk of serious adverse ids. • Do not break, crush, or open
effects; GI bleeding, ulceration. extended-release capsule. Swallow
INTERACTIONS whole.
DRUG: May increase risk of bleeding; ad- IV INCOMPATIBILITIES
verse effects of apixaban, dabigatran, Amino acid injection, calcium gluconate,
edoxaban, rivaroxaban. Bile acid DOBUTamine (Dobutrex), DOPamine
sequestrants (e.g., cholestyramine) (Intropin), gentamicin (Garamycin), to-
may decrease absorption/effect. May bramycin (Nebcin).
increase nephrotoxic effect of cyclo-
SPORINE. May increase concentration/ IV COMPATIBILITIES
effect of lithium. May decrease effect Insulin, potassium.
of loop diuretics (e.g., bumetanide,
furosemide). HERBAL: Glucosamine, INDICATIONS/ROUTES/
herbals with anticoagulant/anti- DOSAGE
platelet properties (e.g., garlic, gin- Moderate to Severe Rheumatoid
ger, ginseng, ginkgo biloba) may in- Arthritis (RA), Osteoarthritis, Ankylosing
crease concentration/effect. FOOD: None Spondylitis
known. LAB VALUES: May prolong PO: ADULTS, ELDERLY, CHILDREN OLDER
bleeding time. May alter serum glucose. THAN 14 YRS: (Immediate-Release): Ini-

Canadian trade name Non-Crushable Drug High Alert drug


600 indomethacin
tially, 25 mg 2–3 times/day; increased SIDE EFFECTS
by 25–50 mg/wk up to 150–200 mg/ Frequent (11%–3%): Headache, nausea,
day. (Extended-Release): Initially, 75 vomiting, dyspepsia, dizziness. Occasional
mg once daily. May increase to 75 mg (less than 3%): Depression, tinnitus,
twice daily. Maximum: 150 mg/day. diaphoresis, drowsiness, constipation,
CHILDREN 2 YRS AND OLDER: (Immediate- diarrhea. Patent ductus arteriosus:
Release): 1–2 mg/kg/day in 2–4 divided Bleeding abnormalities. Rare: Hyperten-
doses. Maximum: 4 mg/kg/day not to sion, confusion, urticaria, pruritus, rash,
exceed 150–200 mg/day. blurred vision.
Acute Gouty Arthritis ADVERSE EFFECTS/TOXIC
PO, rectal: ADULTS, ELDERLY: (Imme- REACTIONS
diate-Release): 50 mg 3 times/day for
Paralytic ileus, ulceration of esophagus,
5–7 days until pain is tolerable, then rap-
stomach, duodenum, small intestine may
idly reduce dose to complete cessation of
occur. Pts with renal impairment may
I medication.
develop hyperkalemia with worsening of
Acute Bursitis, Tendonitis renal impairment. May aggravate depres-
PO: ADULTS, ELDERLY: (Immediate- sion or other psychiatric disturbances,
Release): 75–150 mg/day in 3–4 epilepsy, parkinsonism. Nephrotoxicity
divided doses for 7–14 days. (Ex- (dysuria, hematuria, proteinuria, ne-
tended-Release): 75–150 mg/day in phrotic syndrome) occurs rarely. Meta-
1–2 doses/day for 7–14 days. bolic acidosis/alkalosis, bradycardia oc-
cur rarely in neonates with patent ductus
Acute Pain arteriosus.
20
PO: ADULTS, ELDERLY: (Tivorbex):
mg 3 times/day or 40 mg 2–3 times/ NURSING CONSIDERATIONS
day. BASELINE ASSESSMENT
Patent Ductus Arteriosus Assess onset, type, location, duration of
IV: NEONATES: Initially, 0.2 mg/kg. pain, fever, inflammation. Inspect ap-
Subsequent doses are based on age, pearance of affected joints for immobil-
as follows: NEONATES OLDER THAN 7 ity, deformities, skin condition. Question
DAYS: 0.25 mg/kg for 2nd and 3rd medical history as listed in Precautions.
doses. NEONATES 2–7 DAYS: 0.2 mg/ INTERVENTION/EVALUATION
kg for 2nd and 3rd doses. NEONATES
Monitor serum BUN, creatinine, potas-
YOUNGER THAN 48 HRS: 0.1 mg/kg for
sium, LFT. Monitor for evidence of nau-
2nd and 3rd doses. In general, dos-
sea, dyspepsia. Assist with ambulation if
ing interval is 12 hrs if urine output
dizziness occurs. Evaluate for therapeutic
is greater than 1 mL/kg/hr after prior
response: relief of pain, stiffness, swell-
dose, 24 hrs if urine output is less than 1
ing; increased joint mobility; reduced
mL/kg/hr but greater than 0.6 mL/kg/hr.
joint tenderness; improved grip strength.
Dose is held if urine output is less than
Observe for weight gain, edema, bleed-
0.6 mL/kg/hr or if neonate is anuric.
ing, bruising. In neonates, also monitor
Dosage in Renal Impairment heart rate, heart sounds for murmur, B/P,
Mild to moderate impairment: No urine output, ECG, serum sodium, glu-
dose adjustment. Severe impairment: cose, platelets.
Not recommended. PATIENT/FAMILY TEACHING
Dosage in Hepatic Impairment • Avoid aspirin, alcohol during therapy
Use caution. (increases risk of GI bleeding). • If GI

underlined – top prescribed drug


inFLIXimab 601
upset occurs, take with food, milk. corticosteroid use in moderate to severe
• Avoid tasks that require alertness, mo- active ulcerative colitis.
tor skills until response to drug is estab-
lished. • Report ringing in ears, persis- PRECAUTIONS
tent stomach pain, unusual bruising/ Contraindications: Hypersensitivity to in-
bleeding. FLIXimab. Moderate to severe HF (doses
greater than 5 mg/kg should be avoided).
Sensitivity to murine proteins, sepsis, se-
rious active infection. Cautions: Hema-
inFLIXimab tologic abnormalities, history of COPD,
preexisting or recent-onset CNS demye-
in-flix-i-mab linating disorders, seizures, mild HF, his-
(Remicade, Inflectra, Renflexis) tory of recurrent infections, conditions
j BLACK BOX ALERT jRisk of predisposing pt to infections (e.g., diabe-
severe/fatal opportunistic infec- tes), pts exposed to tuberculosis, elderly
tions (tuberculosis, sepsis, fungal), pts, chronic hepatitis B virus infection. I
reactivation of latent infections.
Rare cases of very aggressive, ACTION
usually fatal hepatosplenic T-cell
lymphoma reported in adolescents, Binds to tumor necrosis factor (TNF), in-
young adults with Crohn’s disease. hibiting functional activity of TNF (induc-
Do not confuse inFLIXimab with tion of proinflammatory cytokines, en-
riTUXimab, or Remicade with hanced leukocytic migration, activation
Reminyl. of neutrophils/eosinophils). Therapeu-
tic Effect: Prevents disease and allows
uCLASSIFICATION diseased joints to heal.
PHARMACOTHERAPEUTIC: Tumor
necrosis factor (TNF) blocking agent. PHARMACOKINETICS
Monoclonal antibody. CLINICAL: An- Absorbed into GI tissue; primarily dis-
tirheumatic, disease-­modifying, GI, tributed in vascular compartment. Half-
immunosuppressant agent. life: 8–9.5 days.
LIFESPAN CONSIDERATIONS
USES Pregnancy/Lactation: Unknown if dis-
In combination with methotrexate, re- tributed in breast milk. Children: Safety
duces signs/symptoms, inhibits progres- and efficacy not established. Elderly: Use
sion of structural damage, improves physi- cautiously due to higher rate of infection.
cal function in moderate to severe active
rheumatoid arthritis (RA). Treatment of INTERACTIONS
psoriatic arthritis. Reduces signs/symp- DRUG: Anakinra, anti-TNF agents,
toms, induces and maintains remission in baricitinib, pimecrolimus, riTUX-
moderate to severe active Crohn’s disease. imab, tacrolimus (topical), tocili-
Reduces number of draining enterocuta- zumab may increase adverse effects.
neous/rectovaginal fistulas, maintains fis- May decrease therapeutic effect of BCG
tula closure in fistulizing Crohn’s disease. (intravesical), vaccines (live). May
Reduces sign/symptoms of active ankylos- increase levels, adverse effects of belim-
ing spondylitis. Treatment of chronic se- umab, natalizumab, tofacitinib, vac-
vere plaque psoriasis in pts who are can- cines (live). HERBAL: Echinacea may
didates for systemic therapy. Reduces sign/ decrease effects. FOOD: None known.
symptoms, induces and maintains clinical LAB VALUES: May increase serum alka-
remission and mucosal healing, eliminates line phosphatase, ALT, AST, bilirubin.

Canadian trade name Non-Crushable Drug High Alert drug


602 inFLIXimab

AVAILABILITY (Rx) adults who respond then lose response,


consideration may be given to treatment
Injection, Powder for Reconstitution: 100 with 10 mg/kg.
mg.
Ankylosing Spondylitis
ADMINISTRATION/HANDLING IV infusion: ADULTS, ELDERLY: 5 mg/
IV kg followed by additional doses at 2 and
6 wks after first infusion, then q6wks
Reconstitution • Reconstitute each
thereafter.
vial with 10 mL Sterile Water for Injection,
using 21-gauge or smaller needle. Direct Psoriatic Arthritis
stream of Sterile Water for Injection to IV infusion: ADULTS, ELDERLY: 5 mg/
glass wall of vial. • Swirl vial gently to kg followed by additional doses at 2 and
dissolve contents (do not shake). • Al- 6 wks after first infusion, then q8wks
low solution to stand for 5 min and inject thereafter. May be used with or without
into 250-mL bag 0.9% NaCl; gently mix. methotrexate.
I Concentration should range between 0.4
and 4 mg/mL. • Begin infusion within 3 Plaque Psoriasis
hrs after reconstitution. IV infusion: ADULTS, ELDERLY: 5 mg/
Rate of administration • Administer kg followed by additional doses at 2 and
IV infusion over at least 2 hrs using a low 6 wks after first infusion, then q8wks
protein-binding filter. thereafter.
Storage • Refrigerate vials. • Solu-
tion should appear colorless to light Ulcerative Colitis
­yellow and opalescent; do not use if dis- IV infusion: ADULTS, ELDERLY, CHIL-
colored or if particulate forms. DREN 6 YRS AND OLDER: 5 mg/kg fol-
lowed by additional doses at 2 and 6
IV INCOMPATIBILITIES wks after first infusion, then q8wks
Do not infuse in same IV line with other thereafter.
agents.
Dosage in Renal/Hepatic Impairment
INDICATIONS/ROUTES/ No dose adjustment.
DOSAGE
SIDE EFFECTS
b ALERT c Premedicate with antihista-
Frequent (22%–10%): Headache, nausea,
mines, acetaminophen, steroids to pre-
vent/manage infusion reactions. fatigue, fever. Occasional (9%–5%): Fe-
ver/chills during infusion, pharyngitis,
Rheumatoid Arthritis (RA) vomiting, pain, dizziness, bronchitis,
IV infusion: ADULTS, ELDERLY: In com- rash, rhinitis, cough, pruritus, sinus-
bination with methotrexate: 3 mg/kg itis, myalgia, back pain. Rare (4%–1%):
followed by additional doses at 2 and 6 Hypotension or hypertension, paresthe-
wks after first infusion, then q8wks there- sia, anxiety, depression, insomnia, diar-
after. Range: 3–10 mg/kg repeated at 4- rhea, UTI.
to 8-wk intervals.
ADVERSE EFFECTS/TOXIC
Crohn’s Disease REACTIONS
IV infusion: ADULTS, ELDERLY, CHILDREN Serious infections, including sepsis, oc-
6 YRS AND OLDER: 5 mg/kg followed by cur rarely. Potential for hypersensitivity
additional doses at 2 and 6 wks after reaction, lupus-like syndrome, severe
first infusion, then q8wks thereafter. For hepatic reaction, HF.

underlined – top prescribed drug


inotuzumab ­ozogamicin 603

NURSING CONSIDERATIONS j BLACK BOX ALERT jHepato-


toxicity, including fatal hepatic
BASELINE ASSESSMENT veno-occlusive disease may occur,
esp. in pts who underwent hemat-
Evaluate baseline hydration status (skin opoietic stem cell transplant (HSCT)
turgor urinary status). Question history or underwent HSCT conditioning
of CNS disorders, COPD, HF. Screen for regimens containing two alkylating
active infection. Pts should be evaluated agents and had a total bilirubin
for active tuberculosis and tested for la- level greater than ULN. Other risk
factors for hepatic veno-occlusive
tent infection prior to initiating treatment disease may include advanced age,
and periodically during therapy. Indura- prior hepatic disease, later salvage
tion of 5 mm or greater with tuberculin lines, greater number of treatment
skin test should be considered a positive cycles. Permanently discontinue
test result when assessing if treatment for in pts who develop hepatic veno-
occlusive disease. LFT elevations
latent tuberculosis is necessary. Verify may require treatment interruption,
that pt has not received live vaccines dose reduction, or permanent dis-
prior to initiation. continuation. Increased occurrence I
of post-HSCT nonrelapse mortality
INTERVENTION/EVALUATION was reported.
Monitor urinalysis, erythrocyte sedi- Do not confuse inotuzumab with
mentation rate (ESR), B/P. Monitor for ado-trastuzumab, alemtuzumab,
signs of infection. Monitor daily pat- atezolizumab, benralizumab,
tern of bowel activity, stool consistency. dinutuximab, elotuzumab,
Crohn’s disease: Monitor C-reactive gemtuzumab, ipilimumab,
protein, frequency of stools. Assess for obinutuzumab, pertuzumab,
abdominal pain. Rheumatoid arthri- trastuzumab.
tis (RA): Monitor C-reactive protein.
uCLASSIFICATION
Assess for decreased pain, swollen
joints, stiffness. PHARMACOTHERAPEUTIC: Anti-
CD22. Antibody drug conjugate
PATIENT/FAMILY TEACHING (ADC). Monoclonal antibody. CLINI-
• Report persistent fever, cough, ab- CAL: Antineoplastic.
dominal pain, swelling of ankles/feet.
• Treatment may depress your immune
system and reduce your ability to fight USES
infection. • Report symptoms of infec- Treatment of adults with relapsed or re-
tion such as body aches, chills, cough, fractory B-cell precursor acute lympho-
fatigue, fever. Avoid those with active in- blastic leukemia (ALL).
fection. • Do not receive live vac-
cines. • Expect frequent tuberculosis PRECAUTIONS
screening. • Report travel plans to pos- Contraindications: Hypersensitivity to
sible endemic areas. inotuzumab. Administration of live vac-
cines. Cautions: Conditions predisposing
to infection (e.g., diabetes, immuno-
compromised pts, renal failure, open
inotuzumab wounds), elderly. Pts at risk for hepatic
­ozogamicin veno-occlusive disease (e.g., advanced
age, prior HSCT, prior hepatic disease
in-oh-tooz-ue-mab oh-zoe-ga- (e.g., cirrhosis, hepatitis), later salvage
mye-sin lines, greater number of treatment cy-
(Besponsa) cles). Pts at risk for QT interval prolon-
gation or torsades de pointes ­(congenital
Canadian trade name Non-Crushable Drug High Alert drug
604 inotuzumab ­ozogamicin
long QT syndrome, medications that prolongation, torsades de pointes. May di-
prolong QT interval, hypokalemia, hypo- minish therapeutic effect of nivolumab.
magnesemia). Pts at risk for hemorrhage May increase adverse effects of natali-
(e.g., history of intracranial/GI bleeding, zumab, vaccines (live). May decrease
coagulation disorders, recent trauma; therapeutic effect of BCG (intravesical),
concomitant use of anticoagulants, anti- vaccines (live). HERBAL: Echina-
platelets, NSAIDS). Pts at risk for tumor cea may decrease concentration/effect.
lysis syndrome (high tumor burden). FOOD: None known. LAB VALUES: May
decrease Hgb, leukocytes, lymphocytes,
ACTION neutrophils, platelets. May increase serum
Binds to and internalizes ADC-CD22 alkaline phosphatase, ALT, amylase AST,
complex in CD22-expressing tumor cells, bilirubin, GGT, lipase, uric acid. May de-
promoting cellular release of N-acetyl- crease diagnostic effect of Coccidioides
gamma-calicheamicin dimethylhydrazide immitis skin test.
(a cytotoxic agent). Activation of N-ace-
I tyl-gamma-calicheamicin dimethylhydra- AVAILABILITY (Rx)
zide induces breakage of double-strand Injection, Powder for Reconstitution:
DNA, resulting in cell cycle arrest and 0.9 mg.
apoptosis. Therapeutic Effect: Inhibits
tumor cell growth and metastasis in ALL. ADMINISTRATION/HANDLING
IV
PHARMACOKINETICS
Widely distributed. N-acetyl-gamma-­ Premedication • Premedicate with a
calicheamicin dimethylhydrazide metabo- corticosteroid, antipyretic, and antihista-
lized by nonenzymatic reduction. P­ rotein mine before each dose.
binding: 97%. Steady state reached by Reconstitution • Must be prepared
treatment cycle 4. Excretion not specified. by personnel trained in aseptic manipu-
Half-life: 12.3 days. lations and admixing of cytotoxic
drugs. • Calculate the number of vials
LIFESPAN CONSIDERATIONS required for dose. • Reconstitute each
Pregnancy/Lactation: Avoid pregnancy;
vial with 4 mL Sterile Water for Injection
may cause fetal harm. Unknown if distrib- for a final concentration of 0.25 mg/mL
uted in breast milk. Females of reproduc- that delivers 3.6 mL (0.9 mg). • Gently
tive potential must use effective contra- swirl vial until completely dis-
ception during treatment and for at least solved. • Do not shake or agi-
8 mos after discontinuation. Males with tate. • Visually inspect for particulate
female partners of reproductive potential matter or discoloration. Solution should
must use effective contraception during appear clear to opalescent, colorless to
treatment and for at least 5 mos after dis- slightly yellow in color. Do not use if so-
continuation. Breastfeeding not recom- lution is cloudy or discolored, or if visi-
mended during treatment and for at least ble particles are observed. • Calculate
2 mos after discontinuation. May impair required volume of reconstituted solu-
fertility in females. Children: Safety and tion according to body surface
efficacy not established. Elderly: No age- area. • Dilute in 50 mL 0.9% NaCl
related precautions noted. polyvinyl chloride (PVC) infusion bag
­
made of (DEHP or non-DEHP), polyole-
INTERACTIONS fin, or ethylene vinyl acetate. • Mix by
DRUG: QT interval–prolonging medi-
gently inversion. Do not shake or agi-
cations (e.g., amiodarone, azithro- tate. • Discard unused portions.
mycin, ciprofloxacin, haloperidol, Rate of administration • Infuse over
sotalol) may increase risk of QT interval 60 min via dedicated IV line. • In-line

underlined – top prescribed drug


inotuzumab ­ozogamicin 605
filters are not required. However, if an Dose Modification
in-line filter is used, filters made of poly- Note: Doses within a treatment cycle
ethersulfone (PES), polyvinylidene fluo- (e.g., day 8, day 15) do not require in-
ride (PVDF), or hydrophilic polysulfone terruption if related to neutropenia or
(HPS) are recommended. Do not use thrombocytopenia. Treatment interrup-
filters made of nylon or mixed cellulose tions within a cycle are recommended
ester (MCE). • Do not administer as IV for nonhematological toxicities. Do not
push or bolus. re-escalate reduced doses that are re-
Storage • Refrigerate unused vials in lated to toxicity.
original carton. • Protect vial, reconsti-
Duration of Dose Interruption
tuted solution, diluted solution from
(Nonhematological Toxicities)
light. • Do not freeze. • Reconstitu-
tion solution must be diluted within 4 Less than 7 days within a cycle: In-
hrs. • Diluted solution may be stored at terrupt the next dose (ensure a minimum
room temperature for up to 4 hrs or re- of 6 days between doses). 7 days or
more: Skip the next dose within the cy- I
frigerated for up to 3 hrs. • If refriger-
ated, allow diluted solution to warm to cle. 14 days or more: Once toxicity is
room temperature (approx. 1 hr). • In- adequately resolved, decrease total dose
fusion must be completed within 8 hrs of of subsequent cycle by 25%. May further
reconstitution. reduce to 2 doses per cycle for subse-
quent cycles if further dose modification
INDICATIONS/ROUTES/ is required. If unable to tolerate a total
DOSAGE dose reduction of 25%, followed by a re-
ALL (Relapsed or Refractory)
duction to 2 doses per cycle, permanently
IV: ADULTS, ELDERLY: Induction cycle
discontinue. More than 28 days: Con-
1: 0.8 mg/m2 on day 1, then 0.5 mg/m2
sider permanent discontinuation.
on day 8 and day 15 of 21-day cycle (total Hematologic Toxicities
cycle dose: 1.8 mg/m2 per cycle, given in ANC greater than or equal to 1,000
3 divided doses). May extend duration of cells/mm3 (prior to treatment): If ANC
induction cycle to 28 days if pt achieves decreases, interrupt next cycle until ANC is
complete remission (CR), complete re- greater than or equal to 1,000 cells/mm3.
mission with incomplete hematologic re- Discontinue treatment if ANC is less than
covery (CRi), or to allow time for recov- 1,000 cells/mm3 for more than 28 days
ery of toxicity. Subsequent cycles in pts (and related to treatment). Platelet count
with CR or CRi: 0.5 mg/m2 on days 1, 8, greater than or equal to 50,000 cells/
and 15 of 28-day cycle (total cycle dose: mm3 (prior to treatment): If platelet
1.5 mg/m2 per cycle, given in 3 divided count decreases, interrupt next cycle until
doses). Subsequent cycles in pts who platelet count is greater than or equal to
have not achieved CR or CRi: 0.8 mg/ 50,000 cells/mm3. Discontinue treatment
m2 on day 1, then 0.5 mg/m2 on day 8 and if platelet count is less than 50,000 cells/
day 15 of 28-day cycle (total cycle dose: mm3 for more than 28 days (and related
1.8 mg/m2 per cycle, given in 3 divided to treatment). ANC less than 1,000
doses). Recommend discontinuation in cells/mm3 and/or platelet count less
pts who do not achieve CR or CRi within 3 than 50,000 cells/mm3 (prior to treat-
cycles. Proceeding to HCST: ­Treatment ment): If ANC or platelet count decreases,
duration of 2 cycles. May consider a third interrupt next cycle until one of following
cycle in pts who do not achieve CR or occurs: ANC and platelet count recover to
Cri and minimal residual disease after 2 at least baseline of the prior cycle; ANC is
cycles. Not proceeding to HCST: May greater than or equal to 1,000 cells/mm3
consider up to a maximum of 6 cycles. and platelet count is greater than or equal

Canadian trade name Non-Crushable Drug High Alert drug


606 inotuzumab ­ozogamicin
to 50,000 cells/mm3; disease is improved be life-­threatening. Hemorrhagic events
or stable, and the decrease of ANC and including contusion, ecchymosis, epi-
platelet count is not related to treatment. staxis, gingival bleeding, hematemesis,
hematochezia, hematotympanum, hema-
Hepatotoxicity
turia, metrorrhagia, subdural hematoma,
Serum ALT/AST greater than 2.5 times
postprocedural hematoma, hemorrhagic
ULN and serum bilirubin greater than
shock, hemorrhage (conjunctival, gas-
1.5 times ULN: Interrupt treatment until
tric, GI, hemorrhoidal, intra-abdominal,
serum ALT/AST is less than or equal to 2.5 intracranial, lip, mesenteric, mouth,
times ULN and serum bilirubin is less than muscle, rectal, SQ, vaginal) have oc-
1.5 times ULN prior to each dose (unless curred. Hepatotoxicity, including fatal
related to Gilbert’s syndrome or hemodialy- hepatic veno-occlusive disease, may oc-
sis). Permanently discontinue if serum ALT/ cur, esp. in pts who underwent HSCT or
AST does not recover to less than or equal to underwent HSCT conditioning regimens
2.5 times ULN or serum bilirubin does not containing two alkylating agents and had
I recover to less than 1.5 times ULN. Hepatic a total bilirubin level greater than ULN.
veno-occlusive disease, severe liver
An increased occurrence of post-HSCT
injury: Permanently discontinue.
nonrelapse mortality was reported. Seri-
Other Nonhematologic Toxicities ous, sometimes fatal, infections including
Any CTCAE Grade 2 nonhemato- neutropenic sepsis, pneumonia, sepsis,
logic toxicities: Withhold treatment pseudomonal sepsis occurred in 5% of
until recovery to Grade 1 or pretreatment pts. Tumor lysis syndrome may present as
grade levels before each dose. acute renal failure, hypocalcemia, hyper-
uricemia, hyperphosphatemia. May cause
Dosage in Renal Impairment QT interval prolongation, esp. in pts with
Mild impairment: No dose adjustment history of long QTc prolongation or in
to initial dose. Severe to moderate im- pts taking medications known to prolong
pairment: Not specified; use caution. QT interval. Immunogenicity (anti-inotu-
Dosage in Hepatic Impairment zumab antibodies) occurred in 3% of pts.
Mild to moderate impairment: No
dose adjustment to initial dose. Severe NURSING CONSIDERATIONS
impairment, ESRD, HD: Use caution. BASELINE ASSESSMENT
SIDE EFFECTS Obtain ANC, CBC, LFT; ECG before each
Frequent (35%–17%): Fatigue, asthenia, dose. Calculate body surface area. Obtain
headache, migraine, sinus headache, py- pregnancy test in females of reproductive
rexia, nausea, abdominal pain, esopha- potential. Assess plans of breastfeed-
geal pain, abdominal tenderness, hepatic ing. Screen for active infection. Assess
pain. Occasional (16%–11%): Constipa- risk for bleeding, hemorrhage, hepatic
tion, vomiting, stomatitis, aphthous ulcer, veno-­occlusive disease, infection, QT
mucosal inflammation, mouth ulceration, prolongation. Due to risk of tumor lysis
oral pain, oropharyngeal pain, chills. syndrome, assess adequate hydration be-
fore initiation. Receive full medication
ADVERSE EFFECTS/TOXIC history and screen for interactions. Offer
REACTIONS emotional support.
Anemia, leukopenia, lymphopenia, INTERVENTION/EVALUATION
neutropenia, thrombocytopenia are ex-
pected responses to therapy, but more Monitor ANC, CBC for myelosuppression.
severe reactions, including bone mar- Monitor ECG for QT interval prolonga-
row failure, febrile neutropenia, may tion. LFTs should be obtained before

underlined – top prescribed drug


insulin 607
each dose and correlated with symptoms iting. • Avoid pregnancy using effective
of hepatic veno-occlusive disease (as- contraception. Treatment may cause fetal
cites, serum bilirubin elevation, hepa- harm. Do not breastfeed during treat-
tomegaly, rapid weight gain). Diligently ment and for at least 2 mos after last
monitor pts who underwent HSCT or dose. • Life-threatening bleeding may
are planning HSCT. Monitor for infusion- occur; report bloody stool, bloody urine;
related reactions (e.g., chills, dyspnea, rectal bleeding, nosebleeds, vomiting up
fever, rash) during infusion and for at blood; symptoms of hemorrhagic stroke
least 1 hr after infusion is completed. If (confusion, blindness, difficulty speak-
infusion-related reaction occurs during ing, paralysis, seizures). • Do not take
administration, interrupt infusion and any newly prescribed medications unless
provide medical support. Severe reac- approved by doctor who originally
tions may require administration of anti- started treatment. • Report symptoms
histamines, corticosteroids. Permanently of long QT syndrome such as chest pain,
discontinue t­reatment if severe or life- dizziness, fainting, palpitations, short-
threatening reactions occur. Be alert for ness of breath. • Report liver problems I
serious infection, opportunistic infection, such as abdominal pain, bruising, clay-
sepsis (fever, decreased urinary output, colored stool, amber or dark-colored
hypotension, tachycardia, t­achypnea). If urine, yellowing of the skin or
infection occurs, provide anti-infective eyes. • Pts who have had HSCT or are
therapy as appropriate. Monitor for planning HSCT have an increased risk of
hemorrhagic events including intra- mortality.
cranial hemorrhage (altered mental
status, aphasia, blindness, hemiparesis,
unequal pupils, seizures), GI bleeding
(hematemesis, melena, rectal bleeding), insulin
epistaxis. Tumor lysis syndrome may
present as acute renal failure, hypocalce- in-su-lin
mia, hyperuricemia, hyperphosphatemia. Do not confuse NovoLOG with
Monitor daily pattern of bowel activity, HumaLOG or NovoLIN.
stool ­consistency. Rapid-acting: (Afrezza): INHALATION
POWDER, INSULIN ASPART: (Fiasp,
PATIENT/FAMILY TEACHING
NovoLOG), INSULIN GLULISINE: (Api-
• Treatment may depress your immune dra), INSULIN LISPRO: (HumaLOG)
system response and reduce your ability Short-acting: REGULAR INSULIN: (Hu-
to fight infection. Report symptoms of muLIN R , NovoLIN R) Intermediate-
infection such as body aches, chills, acting: NPH: (HumuLIN N , NovoLIN N)
cough, fatigue, fever. Avoid those with Long-acting: INSULIN DEGLUDEC:
active infection. • Report symptoms of (Tresiba), INSULIN DETEMIR:
bone marrow depression such as bruis- (Levemir), INSULIN GLARGINE: (Basa-
ing, fatigue, fever, shortness of breath, glar, Lantus , Toujeo)
weight loss; bleeding easily, bloody urine j BLACK BOX ALERT j (Afrez-
or stool. • Therapy may cause life- za): Acute bronchospasms reported
threatening tumor lysis syndrome (a in pts with asthma and COPD.
condition caused by the rapid break-
down of cancer cells), which can cause FIXED-COMBINATION(S)
kidney failure. Report decreased urina- HumaLOG Mix 75/25: lispro sus-
tion, amber-colored urine; confusion, pension 75% and lispro solution 25%.
difficulty breathing, fatigue, fever, muscle HumuLIN Mix 50/50: NPH 50% and
or joint pain, palpitations, seizures, vom- regular 50%. HumuLIN 70/30, No-

Canadian trade name Non-Crushable Drug High Alert drug


608 insulin
voLIN 70/30: NPH 70% and rapid- triglyceride synthesis. Therapeutic Ef-
acting regular 30%. NovoLOG Mix fect: Controls serum glucose levels.
70/30: aspart suspension 70% and
aspart solution 30%. Ryzodeg 70/30: PHARMACOKINETICS
degludec suspension 70% and aspart Rapid-Acting
solution 30%. Soliqua 100/33: Onset Peak Duration
glargine 100 units/mL and lixisenatide (min) (hrs) (hrs)
(a glucagon-like peptide 1 [GLP-1] re- Fiasp 12–18 1.5–2.2 5–7
ceptor agonist) 33 mcg/mL. Xultophy Aspart 10–20 1–3 3–5
100/3.6: degludec 100 units/mL and ­(NovoLOG)
liraglutide (a GLP-1 receptor agonist) Glulisine 5–15 0.75– 2–4
3.6 mg/mL. ­(Apidra) 1.25
Insulin Human 15–30 1 2
uCLASSIFICATION (Afrezza)
Lispro 15–30 0.5–2.5 3–6.5
PHARMACOTHERAPEUTIC: Exog- ­(HumaLOG)
I enous insulin. CLINICAL: Antidia-
betic. Short-Acting
Onset Peak Duration
(min) (hrs) (hrs)
USES Regular 30–60 1–5 6–10
Treatment of type 1 diabetes (insulin- ­(HumuLIN R)
dependent) and type 2 diabetes (non– Regular 30–60 1–5 6–10
insulin-dependent) to improve glycemic ­(NovoLIN R)
control. OFF-LABEL: Insulin aspart,
Intermediate-Acting
insulin lispro, insulin regular: Ges-
tational diabetes, mild to moderate dia- Onset Peak Duration
betic ketoacidosis, mild to moderate hy- (hrs) (hrs) (hrs)
perosmolar hyperglycemic state. Insulin NPH 1–2 6–14 16–24+
NPH: Gestational diabetes. (HumuLIN N)
NPH 1–2 6–14 16–24+
PRECAUTIONS (NovoLIN N)

Contraindications: Hypersensitivity to insu- Long-Acting


lin, use during episodes of hypoglycemia. Onset Duration
Afrezza: Chronic lung disease. Cau- (hrs) Peak (hrs) (hrs)
tions: Pts at risk for hypokalemia; renal/he- Degludec 0.5–1.5 12 42
patic impairment, elderly. Afrezza: Must (Tresiba)
be used with a long-acting insulin in type 1 Detemir 3–4 3–9 6–23
diabetes. Not recommended for use in dia- (Levemir)
betic ketoacidosis or in smokers. Pts with Glargine 3–4 No peak 24
active lung cancer, history of lung cancer, (Lantus)
or at risk for lung cancer. Glargine Over 6 No peak Over 24
(Toujeo)
ACTION
Acts via specific receptor to regulate me- LIFESPAN CONSIDERATIONS
tabolism of carbohydrates, protein, and Pregnancy/Lactation: Insulin is the
fats. Acts on liver, skeletal muscle, and drug of choice for diabetes in pregnancy;
adipose tissue. Liver: Stimulates hepatic close medical supervision is needed. Fol-
glycogen synthesis, synthesis of fatty ac- lowing delivery, insulin needs may drop
ids. Muscle: Increases protein, glycogen for 24–72 hrs, then rise to pre­pregnancy
synthesis. Adipose tissue: Stimulates levels. Not distributed in breast
lipoproteins to provide free fatty acids, milk; lactation may decrease i­nsulin
underlined – top prescribed drug
insulin 609
­requirements. Children: No age-related Intermediate- and Short-Acting Mixtures:
precautions noted. Elderly: Decreased HumuLIN 50/50, HumuLIN 70/30, Hum-
vision, fine motor tremors may lead to aLOG Mix 75/25, HumaLOG Mix 50/50,
inaccurate self-dosing. NovoLIN 70/30, NovoLOG Mix 70/30.

INTERACTIONS ADMINISTRATION/HANDLING
DRUG: Alcohol may increase risk of IV
hypoglycemia. Beta blockers (e.g.,
carvedilol, metoprolol) may alter ef- Regular and Insulin Glulisine:
fects; may mask signs, prolong periods of • (Apidra): Use only if solution is clear.
hypoglycemia. glucagon-like peptide • May give undiluted.
1 (GLP-1) agents (e.g., liraglutide),
dipeptidyl peptidase (DPP)-4 agents Rapid-Acting • (Afrezza): Administer
(e.g., linagliptin), thiazolidine­ using a single inhalation/cartridge. Give
diones (e.g., pioglitazone), pram- at beginning of a meal. • (Aspart
lintide may increase hypoglycemic [NovoLOG]): May give SQ, IV I
effect. HERBAL: Herbals with hypogly- infusion. • Can mix with NPH
cemic properties (e.g., fenugreek) (draw aspart into syringe first; inject
may increase hypoglycemic effect. immediately after mixing). • After first
FOOD: None known. LAB VALUES: May use, stable at room temperature for 28
decrease serum magnesium, phosphate, days. • Administer 5–10 min before
potassium. meals. • Glulisine (Apidra): May mix
with NPH (draw glulisine into syringe first;
AVAILABILITY (RX) inject immediately after mixing). • After
Rapid-Acting first use, stable at room temperature
Inhalation Powder: (Afrezza): 4 units, 8 for 28 days. • Administer 15 min
units, 12 units as single-use inhalation before or within 20 min after starting a
cartridges. Aspart (NovoLOG): 100 units/ meal. • (Lispro [HumaLOG]): For SQ
mL vial, 3-mL cartridge, 3-mL Flex-Pen. use only. • May mix with NPH. Stable for
Glulisine (Apidra): 100 units/mL vial, 28 days at room temperature; syringe is
3-mL cartridge. Lispro (HumaLOG): 100 stable for 14 days if refrigerated. • After
units/mL vial, 3-mL cartridge, 3-mL pen. first use, stable at room temperature for
28 days. • Administer 15 min before or
Short-Acting immediately after meals.
Regular: (HumuLIN R): 100 units/mL
vial, U-500 Kwik Pen. Regular: (NovoLIN Short-Acting
R): 100 units/mL vial, 3-mL cartridge, Regular • (HumuLIN R, NovoLIN
3-mL Innolet prefilled syringe. R): May give SQ, IM, IV. • May mix
Intermediate-Acting
with NPH for immediate use or for
NPH: (HumuLIN N): 100 units/mL vial,
storage for future use. Stable for
3-mL pen. NPH: (NovoLIN N): 100 units/ 1 mo at room temperature, 3 mos
mL vial, 3-mL cartridge, 3-mL Innolet if refrigerated. • Can mix with
prefilled syringe. Sterile Water for Injection or 0.9%
NaCl. • After first use, stable at room
Long-Acting temperature for 28 days. • Administer
Detemir: (Levemir): 100 units/mL vial, 30 min before meals.
3-mL Flex-Pen. Glargine: (Lantus): 100
units/mL vial, 3-mL cartridge. Glargine: Intermediate-Acting
(Toujeo SoloStar): 300 units/mL. (Basa- NPH • (HumuLIN N, NovoLIN N):
glar KwikPen): 100 units/mL. For SQ use only. • May mix with as-

Canadian trade name Non-Crushable Drug High Alert drug


610 insulin
part (NovoLOG) or lispro (HumaLOG). digoxin (Lanoxin), DOBUTamine (Do-
Draw aspart or lispro first and use im- butrex), famotidine (Pepcid), genta-
mediately. • May mix with regular micin, heparin, magnesium sulfate,
(HumuLIN R, NovoLIN R) insulin. Draw metoclopramide (Reglan), midazolam
regular insulin first, use immediately (Versed), milrinone (Primacor), mor-
or may store for future use (up to 28 phine, nitroglycerin, potassium chlo-
days). • After first use, stable at room ride, propofol (Diprivan), vancomycin
temperature for 28 days. • Administer (Vancocin).
15 min before meals when mixed with
aspart or lispro; 30 min before meals INDICATIONS/ROUTES/DOSAGE
when mixed with regular ­insulin. Note: Insulin requirements vary dra-
matically among pts, requiring dosage
Long-Acting adjustment.
• (Degludec [Tresiba]): For SQ use
only. • Do not mix with other insu- Type 1 Diabetes
I lins. • After first use, stable at room Multiple daily injections, guided by
temperature for 56 days. • May take glucose monitoring or continuous SQ
once daily any time of day. • (Detemir insulin infusions, is standard of care.
[Levemir]): For SQ use only. • Do Usual initial dose: 0.4–0.5 unit/kg/
not mix with other insulins. • After day in divided doses. Usual mainte-
first use, stable at room temperature nance: 0.4–1 units/kg/day in divided
for 42 days. • Evening dose given at doses.
dinner or at bedtime. Twice-daily regi-
mens can be given 12 hrs after morning Type 2 Diabetes
dose. • (Glargine [Lantus, Toujeo]): Initially, 4–6 units or 0.1–0.2 units/
For SQ use only. • Do not mix with other kg given before largest meal of day.
insulins. • After first use, stable at room Adjust dose by 2 units q3days to reach
temperature for 28 days. • Administer fasting glucose target (while avoid-
once daily at same time. Meal timing is not ing hypoglycemia). General goal is
applicable. to achieve Hgb A1c less than 7% using
safe medication titration. Dual therapy
SQ (metformin and a second antihyper-
• Check serum glucose concentration be- glycemic agent) is recommended in
fore administration; dosage highly individu- pts who fail to achieve glycemic goals
alized. • SQ injections may be given in after 3 mos with lifestyle interven-
thigh, abdomen, upper arm, buttocks, up- tions and metformin monotherapy.
per back if there is adequate adipose tis- (Afrezza): Dosage based on meta-
sue. • Rotation of injection sites is essen- bolic needs, blood glucose results,
tial; maintain careful record. • Prefilled glycemic goal control.
syringes should be stored in vertical or
oblique position to avoid plugging; plunger Dosage in Renal Impairment
should be pulled back slightly and syringe Creatinine
rocked to remix solution before injection. Clearance Dose
IV INCOMPATIBILITIES 10–50 mL/min 75% normal dose
Less than 10 mL/min 25%–50% normal
DilTIAZem (Cardizem), DOPamine (In- dose
tropin), nafcillin (Nafcil).
Dosage in Hepatic Impairment
IV COMPATIBILITIES Insulin requirement may be reduced.
Amiodarone (Cordarone), ampicillin/
sulbactam (Unasyn), ceFAZolin (Ancef),

underlined – top prescribed drug


interferon alfa-2b 611

SIDE EFFECTS PATIENT/FAMILY TEACHING


Occasional: Localized redness, swelling, • Instruct on proper technique for drug
itching (due to improper insulin injection administration, testing of glucose, signs/
technique), allergy to insulin ­ cleansing symptoms of hypoglycemia and hyperglyce-
solution. Infrequent: ­Somogyi effect (re- mia. • Diet and exercise are essential
bound hyperglycemia) with ­ chronically parts of treatment; do not skip/delay
excessive insulin dosages. Systemic allergic meals. • Carry candy, sugar packets,
reaction (rash, angioedema, anaphylaxis), other sugar supplements for immediate re-
lipodystrophy (depression at injection site sponse to hypoglycemia. • Wear or carry
due to breakdown of adipose tissue), lipo- medical alert identification. • Check with
hypertrophy (accumulation of SQ tissue at physician when insulin demands are al-
injection site due to inadequate site rota- tered (e.g., fever, infection, trauma, stress,
tion). Rare: Insulin resistance. heavy physical activity). • Do not take
other medication without consulting physi-
ADVERSE EFFECTS/TOXIC cian. • Weight control, exercise, hygiene
REACTIONS (including foot care), not smoking are inte- I
Severe hypoglycemia (due to hyperinsu- gral parts of therapy. • Protect skin, limit
linism) may occur with insulin overdose, sun exposure. • Inform dentist, physi-
decrease/delay of food intake, excessive cian, surgeon of medication before any
exercise, pts with brittle diabetes. Dia- treatment is given.
betic ketoacidosis may result from stress,
illness, omission of insulin dose, long-
term poor insulin control.
NURSING CONSIDERATIONS interferon alfa-2b
BASELINE ASSESSMENT
Obtain serum glucose level, Hgb A1c. in-ter-feer-on
Discuss lifestyle to determine extent of (Intron-A)
learning, emotional needs. If given IV, j BLACK BOX ALERT jMay
cause or aggravate fatal or life-
obtain serum chemistries (esp. serum threatening autoimmune disorders,
potassium). ischemia, neuropsychiatric symp-
toms (profound depression, suicidal
INTERVENTION/EVALUATION thoughts/behaviors), infectious
Assess for hypoglycemia (refer to phar- disorders.
macokinetics table for peak times and Do not confuse interferon
duration): cool, wet skin, tremors, diz- alfa-2b with interferon alfa-2a,
ziness, headache, anxiety, tachycardia, interferon alfa-n3, or peginter-
numbness in mouth, hunger, diplopia. feron alfa-2b, or Intron with
Assess sleeping pt for restlessness, dia- Peg-Intron.
phoresis. Check for hyperglycemia: poly-
uria (excessive urine output), polypha- FIXED-COMBINATION(S)
gia (excessive food intake), polydipsia Rebetron: interferon alfa-2b/ribavirin
(excessive thirst), nausea/vomiting, dim (an antiviral): 3 million units/200 mg.
vision, fatigue, deep and rapid breathing
(Kussmaul respirations). Be alert to con- uCLASSIFICATION
ditions altering glucose requirements: PHARMACOTHERAPEUTIC: Biologic
fever, trauma, increased activity/stress, response modifier, immunomodula-
surgical procedure. tor. CLINICAL: Antineoplastic.

Canadian trade name Non-Crushable Drug High Alert drug


612 interferon alfa-2b

USES LIFESPAN CONSIDERATIONS


Treatment of hairy cell leukemia, condylo- Pregnancy/Lactation: If possible,
mata acuminata (genital, venereal warts), avoid use during pregnancy. Breastfeed-
malignant melanoma, AIDS-related Ka- ing not recommended. Children: Safety
posi’s sarcoma, chronic hepatitis C virus and efficacy not established. El-
infection (including children 3 yrs of age derly: Neurotoxicity, cardiotoxicity may
and older), chronic hepatitis B virus infec- occur more frequently. Age-related renal
tion (including children 1 yr and older), impairment may require dosage adjust-
follicular non-Hodgkin’s lymphoma. OFF- ment.
LABEL: Treatment of bladder, cervical,
renal carcinoma; chronic myelocytic leu- INTERACTIONS
kemia; laryngeal papillomatosis; multiple DRUG: Bone marrow depressants
myeloma; cutaneous T-cell lymphoma; (e.g., cladribine) may increase myelo-
mycosis fungoides; West Nile virus. suppression. May increase concentra-
tion/effect of tiZANidine. HERBAL: None
I PRECAUTIONS significant. FOOD: None known. LAB
Contraindications: Hypersensitivity to in- VALUES: May increase PT, aPTT, LDH,
terferon alfa-2b. Decompensated hepatic serum alkaline phosphatase, ALT, AST.
disease, autoimmune hepatitis. In com- May decrease Hgb, Hct, leukocyte, plate-
bination with ribavirin: Women who let counts.
are pregnant, men with pregnant part-
ners, pts with hemoglobinemias (e.g., AVAILABILITY (Rx)
sickle cell anemia), CrCl less than 50 mL/ Injection, Powder for Reconstitution: 10
min). Cautions: Renal/hepatic impair- million units, 18 million units, 50 mil-
ment, seizure disorder, compromised lion units.
CNS function, cardiac diseases, myelo- Injection, Solution: 6 million units/mL,
suppression, concurrent use of medica- 10 million units/mL.
tions causing myelosuppression, pul-
monary impairment, multiple sclerosis, ADMINISTRATION/HANDLING
diabetes, thyroid disease, coagulopathy, IV
hypertension, preexisting eye disorders,
history of psychiatric disorders. History Reconstitution • Prepare immediately
of autoimmune disorders, MI, arrhyth- before use. • Reconstitute with diluent
mias, cardiac abnormalities. provided by manufacturer. • Withdraw
desired dose and further dilute with 100
ACTION mL 0.9% NaCl to provide final concentra-
Binds to a specific receptor on cell mem- tion of at least 10 million international
brane to initiate intracellular activity, includ- units/100 mL.
ing suppression of cell proliferation, aug- Rate of administration • Administer
menting specific cytotoxicity of lymphocytes over 20 min.
and increasing phagocyte activity. Thera- Storage • Refrigerate unopened vi-
peutic Effect: Prevents rapid growth of als. • Following reconstitution, stable
malignant cells; inhibits hepatitis virus. for 24 hrs if refrigerated.
PHARMACOKINETICS IM, SQ
Well absorbed after IM, SQ administra- IM • Rotate sites. Preferred sites are an-
tion. Undergoes proteolytic degradation terior thigh, deltoid, and superolateral but-
during reabsorption in kidneys. Half- tock. Administer in evening (if possible).
life: 2–3 hrs. SQ • Reconstitute with recommended
amount of Sterile Water for Injection.

underlined – top prescribed drug


interferon alfa-2b 613
Agitate gently; do not shake. Rotate Malignant Melanoma
sites. Preferred sites are anterior thigh, IV: ADULTS: Initially, 20 million units/m2
abdomen (except around navel), outer 5 times/wk for 4 wks. Maintenance: 10
upper arm. million units subcutaneously 3 times/wk
for 48 wks.
IV INCOMPATIBILITIES
D5W. Do not mix with other medications Follicular Non-Hodgkin’s Lymphoma
via Y-site administration. SQ: ADULTS: 5 million units 3 times/wk
for up to 18 mos.
IV COMPATIBILITIES
Dosage in Renal Impairment
0.9% NaCl, lactated Ringer’s. Do not use when combined with ribavirin.
INDICATIONS/ROUTES/ Dosage in Hepatic Impairment
DOSAGE No dose adjustment (see Contraindica-
Hairy Cell Leukemia tions).
IM, SQ: ADULTS: 2 million units/m2 I
3 times/wk on alternating days for up SIDE EFFECTS
to 6 mos. May continue treatment for Frequent: Flu-like symptoms (fever,
sustained response. If severe adverse fatigue, headache, myalgia, anorexia,
reactions occur, modify dose or tempo- chills), rash (hairy cell leukemia, Ka-
rarily discontinue drug. Discontinue for posi’s sarcoma only). Pts with Ka-
disease progression or failure to respond posi’s sarcoma: All previously men-
after 6 months. tioned side effects plus depression,
dyspepsia, dry mouth or thirst, alo-
Condylomata Acuminata pecia, rigors. Occasional: Dizziness,
Intralesional: ADULTS: 1 million units/ pruritus, dry skin, dermatitis, altered
lesion 3 times/wk on alternating days for taste. Rare: Confusion, leg cramps,
3 wks. May administer a second course at back pain, gingivitis, flushing, tremor,
12–16 wks. Use only 10 million–unit vial, anxiety, eye pain.
and reconstitute with no more than 1 mL di-
luent. Maximum: 5 lesions per treatment. ADVERSE EFFECTS/TOXIC
REACTIONS
AIDS-Related Kaposi’s Sarcoma Hypersensitivity reactions occur rarely.
IM, SQ: ADULTS: 30 million units/m2 3 Severe flu-like symptoms appear dose-
times/wk on alternating days. Use only related.
50 million–unit vials. Continue until dis-
ease progression or maximal response NURSING CONSIDERATIONS
achieved after 16 wks. If severe adverse BASELINE ASSESSMENT
reactions occur, modify dose or tempo-
rarily discontinue drug. CBC, blood chemistries, urinalysis, renal
function, LFT should be performed before
Chronic Hepatitis B Virus Infection initial therapy and routinely thereafter.
IM, SQ: ADULTS: 30–35 million units INTERVENTION/EVALUATION
wkly, either as 5 million units/day or 10
million units 3 times/wk for 16 wks. Offer emotional support. Monitor all
SQ: CHILDREN 1–17 YRS: 3 million units/
levels of clinical function (numerous
m2 3 times/wk for 1 wk, then 6 million side effects). Encourage PO intake, par-
units/m2 3 times/wk for 16–24 wks. ticularly during early therapy. Monitor for
Maximum: 10 million units 3 times/wk. worsening depression, suicidal ideation,
associated behaviors.

Canadian trade name Non-Crushable Drug High Alert drug


614 interferon beta-1a
PATIENT/FAMILY TEACHING ACTION
• Clinical response occurs in 1–3 Exact mechanism unknown. Alters ex-
mos. • Flu-like symptoms tend to di- pression and response to surface an-
minish with continued therapy. • Some tigens and may enhance immune cell
symptoms may be alleviated or mini- activity. Therapeutic Effect: Slows pro-
mized by bedtime doses. • Do not have gression of multiple sclerosis.
immunizations without physician’s ap-
proval (drug lowers resistance). • Avoid PHARMACOKINETICS
contact with those who have recently re- Peak serum levels attained 3–15 hrs after
ceived live virus vaccine. • Avoid tasks IM administration. Biologic markers in-
that require alertness, motor skills until crease within 12 hrs and remain elevated
response to drug is established. • Sips for 4 days. Half-life: 10 hrs (Avonex);
of tepid water may relieve dry 69 hrs (Rebif).
mouth. • Report depression, thoughts
of suicide, unusual behavior. LIFESPAN CONSIDERATIONS
I Pregnancy/Lactation: Has abortifa-
cient potential. Unknown if distributed
in breast milk. Children: Safety and
efficacy not established. Elderly: No in-
interferon beta-1a formation available.

in-ter-feer-on
INTERACTIONS
(Avonex, Rebif) DRUG: None significant. HERBAL: None
Do not confuse Avonex with significant. FOOD: None known. LAB VAL-
Avelox, or interferon beta-1a UES: May increase serum glucose, BUN,
with interferon beta-1b. alkaline phosphatase, bilirubin, calcium,
ALT, AST. May decrease Hgb, neutrophil,
uCLASSIFICATION platelet, WBC.
PHARMACOTHERAPEUTIC: Biologic
response modifier. CLINICAL: Multi-
AVAILABILITY (Rx)
ple sclerosis agent. Injection, Powder for Reconstitution:
(Avonex): 30 mcg. Injection Sotion, Pre-
filled Syringe: (Rebif): 22 mcg/0.5 mL,
USES 44 mcg/0.5 mL. (Avonex): 30 mcg/0.5
Treatment of relapsing multiple sclerosis mL. Titration Pack, Prefilled Syringe:
to slow progression of physical disability, (Rebif): 8.8 mcg/0.2 mL, 22 mcg/0.5
decrease frequency of clinical exacerba- mL.
tions.
ADMINISTRATION/HANDLING
PRECAUTIONS IM (Avonex) Syringe
Contraindications: Hypersensitivity to • Refrigerate syringe. • Allow to warm
natural or recombinant interferon, to room temperature before use. • May
human albumin (only for albumin- store up to 7 days at room temperature.
containing products). Cautions: De-
IM (Avonex) Vial
pression, severe psychiatric disorders,
hepatic impairment, increased serum • Refrigerate vials (may store at room
ALT at baseline, alcohol abuse, cardio- temperature up to 30 days). • Follow-
vascular disease, seizure disorders, my- ing reconstitution, may refrigerate again
elosuppression. but use within 6 hrs if refrigerated. • Re-
constitute 30-mcg MicroPin (6.6 million

underlined – top prescribed drug


interferon beta-1b 615
international units) vial with 1.1 mL dilu-
ent (supplied by manufacturer). • Gen- NURSING CONSIDERATIONS
tly swirl to dissolve medication; do not
BASELINE ASSESSMENT
shake. • Discard if discolored or par-
ticulate forms. • Discard unused por- Obtain CBC, BMP, LFT. Assess home situa-
tion (contains no preservative). tion for support of therapy.
INTERVENTION/EVALUATION
SQ (Rebif)
• Refrigerate. May store at room tempera- Assess for headache, flu-like symptoms,
ture up to 30 days. Avoid heat, light. • Ad- myalgia. Periodically monitor lab results,
minister at same time of day 3 days each re-evaluate injection technique. Assess
wk. Separate doses by at least 48 hrs. for depression, suicidal ideation.
PATIENT/FAMILY TEACHING
INDICATIONS/ROUTES/
DOSAGE • Do not change schedule, dosage with-
out consulting physician. • Follow
Relapsing Multiple Sclerosis
guidelines for reconstitution of product I
IM: (Avonex): ADULTS: 30 mcg once
wkly. and administration, including aseptic
SQ: (Rebif): ADULTS: Target dose 44 technique. • Use puncture-resistant
mcg 3 times/wk: Initially, 8.8 mcg container for used needles, syringes; dis-
3 times/wk for 2 wks, then 22 mcg 3 pose of used needles, syringes prop-
times/wk for 2 wks, then 44 mcg 3 times/ erly. • Injection site reactions may oc-
wk thereafter. Target dose 22 mcg 3 cur. These do not require discontinuation
times/wk: Initially, 4.4 mcg 3 times/wk of therapy, but type and extent should be
for 2 wks, then 11 mcg 3 times/wk for 2 carefully noted. Report flu-like symptoms
wks, then 22 mcg 3 times/wk thereafter. (fever, chills, fatigue, muscle aches).

Dosage in Renal Impairment


No dose adjustment.
Dosage in Hepatic Impairment (Rebif)
Use with caution in pts with history of ac-
interferon beta-1b
tive hepatic disease or ALT more than 2.5 in-ter-feer-on
times upper limit of normal (ULN). (Betaseron, Extavia)
SIDE EFFECTS Do not confuse interferon beta-
1b with interferon beta-1a.
Frequent (67%–11%): Headache, flu-like
symptoms, myalgia, upper respiratory uCLASSIFICATION
tract infection, depression with suicidal PHARMACOTHERAPEUTIC: Biologic
ideation, generalized pain, asthenia, response modifier. CLINICAL: Multi-
chills, sinusitis, infection. Occasional ple sclerosis agent.
(9%–4%): Abdominal pain, arthralgia,
chest pain, dyspnea, malaise, syncope.
Rare (3%): Injection site reaction, hyper- USES
sensitivity reaction. Reduces frequency of clinical exacer-
ADVERSE EFFECTS/TOXIC bations in pts with relapsing-remitting
REACTIONS multiple sclerosis (recurrent attacks of
neurologic dysfunction).
Anemia occurs in 8% of pts. Hepatic fail-
ure has been reported.

Canadian trade name Non-Crushable Drug High Alert drug


616 interferon beta-1b

PRECAUTIONS 0.3-mg (9.6 million international units)


Contraindications: Hypersensitivity to al- vial with 1.2 mL diluent (supplied by
bumin, interferon. Cautions: Depression, manufacturer) to provide concentration
severe psychiatric disorders, hepatic/ of 0.25 mg/mL (8 million units/
renal impairment, alcohol abuse, cardio- mL). • Gently swirl to dissolve medica-
vascular disease, seizure disorders, my- tion; do not shake. • Withdraw 1 mL
elosuppression, pulmonary disease. solution and inject subcutaneously into
arms, abdomen, hips, thighs using
ACTION 27-gauge needle. • Discard unused
Exact mechanism unknown. Immuno- portion (contains no preservative).
modulator effects include enhanced
INDICATIONS/ROUTES/
suppression of T-cell activity, reduced
DOSAGE
pro-inflammatory cytokines, reduced
movement of lymphocytes into CNS. Relapsing-Remitting Multiple Sclerosis
Therapeutic Effect: Improves MRI le- SQ: ADULTS: Initially, 0.0625 mg (0.25
I sions, decreases relapse rate and disease mL) every other day; gradually i­ncrease
severity in multiple sclerosis. by 0.0625 mg every 2 wks. Target dose:
0.25 mg every other day.
PHARMACOKINETICS
Dosage in Renal/Hepatic Impairment
Slowly absorbed following SQ administra-
No dose adjustment.
tion. Half-life: 8 min–4.3 hrs.
SIDE EFFECTS
LIFESPAN CONSIDERATIONS
Frequent (85%–21%): Injection site re-
Pregnancy/Lactation: Spontaneous
action, headache, flu-like symptoms,
abortions reported. Discontinuation of
fever, asthenia, myalgia, sinusitis, diar-
the drug before conception is recom-
rhea, dizziness, altered mental status,
mended. Unknown if distributed in breast
constipation, diaphoresis, vomiting. Oc-
milk. Children: Safety and efficacy not
casional (15%–4%): Malaise, drowsiness,
established. Elderly: No information
alopecia.
available.
ADVERSE EFFECTS/TOXIC
INTERACTIONS REACTIONS
DRUG: None significant. HERBAL: None
Seizures occur rarely.
significant. FOOD: None known. LAB
VALUES: May increase bilirubin, ALT, NURSING CONSIDERATIONS
AST. May decrease neutrophil, lympho-
cyte, WBC. BASELINE ASSESSMENT
Obtain CBC, BMP, LFT. Assess home situa-
AVAILABILITY (Rx) tion for support of therapy.
Injection, Powder for Reconstitution:
INTERVENTION/EVALUATION
0.3 mg.
Periodically monitor lab results, re-
ADMINISTRATION/HANDLING evaluate injection technique. Assess for
SQ nausea (high incidence). Monitor sleep
• Store vials at room tempera- pattern. Monitor daily pattern of bowel
ture. • After reconstitution, stable for 3 activity, stool consistency. Assist with
hrs if refrigerated. • Use within 3 hrs of ambulation if dizziness occurs. Monitor
reconstitution. • Discard if discolored food intake.
or precipitate forms. • Reconstitute

underlined – top prescribed drug


interleukin-2 (aldesleukin) 617
PATIENT/FAMILY TEACHING lasting more than 72 hrs, pts who have
• Report flu-like symptoms (fever, chills, had an organ allograft, cardiac tampon-
fatigue, muscle aches); occur commonly ade, renal dysfunction requiring dialy-
but decrease over time. • Wear sun- sis for longer than 72 hrs, repetitive or
screen, protective clothing if exposed to difficult-to-control seizures; retreatment
sunlight, ultraviolet light until tolerance in pts who experience any of the fol-
known. lowing toxicities: angina, MI, recurrent
chest pain with ECG changes, sustained
ventricular tachycardia, uncontrolled
or unresponsive cardiac rhythm distur-
interleukin-2 bances. Extreme Caution: Pts with nor-
mal thallium stress tests and pulmonary
(aldesleukin) function tests who have history of cardiac
or pulmonary disease. Cautions: Pts with
in-ter-loo-kin fixed requirements for large volumes of
(Proleukin) fluid (e.g., those with hypercalcemia), I
j BLACK BOX ALERT jHigh-dose history of seizures, renal/hepatic impair-
therapy is associated with capillary ment, autoimmune disease, inflammatory
leak syndrome resulting in sig-
nificant hypotension and reduced disorders.
organ perfusion. Use restricted to
pts with normal cardiac/pulmonary ACTION
function. Increased risk of dissemi- Promotes proliferation, differentiation,
nated infection (sepsis, bacterial recruitment of T and B cells, natural
endocarditis). Withhold treatment killer cells, thymocytes. Therapeutic Ef-
for pts developing moderate-to-se-
vere lethargy or drowsiness (contin- fect: Enhances cytolytic activity in lym-
ued treatment may result in coma). phocytes and subsequent interaction be-
Must be administered by personnel tween the immune system and malignant
trained in administration/handling of cells. Can stimulate lymphokine-activated
chemotherapeutic agents. killer (LAK) cells and tumor-infiltrating
Do not confuse aldesleukin with lymphocyte cells..
oprelvekin.
PHARMACOKINETICS
uCLASSIFICATION
Primarily distributed into plasma, lym-
PHARMACOTHERAPEUTIC: Biologic phocytes, lungs, liver, kidney, spleen.
response modifier. CLINICAL: Anti- Metabolized to amino acids in cells lining
neoplastic. the kidneys. Half-life: 80–120 min.
LIFESPAN CONSIDERATIONS
USES Pregnancy/Lactation: Avoid use in
Treatment of metastatic renal cell carci- those of either sex not practicing effective
noma, metastatic melanoma. OFF-LABEL: contraception. Children: Safety and effi-
Treatment of acute myeloid leukemia cacy not established. Elderly: Age-­related
(AML). renal impairment may require dosage ad-
justment; will not tolerate toxicity.
PRECAUTIONS
Contraindications: Hypersensitivity to INTERACTIONS
aldesleukin. Abnormal pulmonary func- DRUG: Corticosteroids (e.g., dexa-
tion or thallium stress test results, bowel methasone, predniSONE) may decrease
ischemia or perforation, coma or toxic therapeutic effect. Cladribine may increase
psychosis lasting longer than 48 hrs, GI myelosuppressive effect. HERBAL: Herb-
bleeding requiring surgery, intubation als with hypotensive properties (e.g.,

Canadian trade name Non-Crushable Drug High Alert drug


618 interleukin-2 (aldesleukin)
garlic, ginger, ginkgo biloba) may al- IV INCOMPATIBILITIES
ter effects. FOOD: None known. LAB VAL- Ganciclovir (Cytovene), pentamidine
UES: May increase serum BUN, alkaline (Pentam), prochlorperazine (Compa-
phosphatase, bilirubin, creatinine, ALT, zine), promethazine (Phenergan).
AST. May decrease serum calcium, mag-
nesium, phosphorus, potassium, sodium. IV COMPATIBILITIES
Calcium gluconate, DOPamine (Intro-
AVAILABILITY (Rx) pin), heparin, LORazepam (Ativan),
Injection, Powder for Reconstitution: (Pro- magnesium, potassium.
leukin): 22 million units (1.3 mg) (18
million units/mL = 1.1 mg/mL when re- INDICATIONS/ROUTES/
constituted). DOSAGE
Metastatic Melanoma, Metastatic Renal
ADMINISTRATION/HANDLING Cell Carcinoma
b ALERT c Hold administration in pts IV: ADULTS 18 YRS AND OLDER: 600,000
I units/kg q8h for 14 doses; followed by 9
who develop moderate to severe lethargy
or drowsiness (continued administration days of rest, then another 14 doses for a
may result in coma). total of 28 doses per course. Course may
be repeated if tumor shrinkage observed
IV after rest period of at least 7 wks from
date of hospital discharge.
Reconstitution • Reconstitute 22
million units vial with 1.2 mL Sterile Wa- Dosage in Renal/Hepatic Impairment
ter for Injection to provide concentration No dose adjustment. Do not initiate if se-
of 18 million units/mL (1.1 mg/ rum creatinine greater than 1.5 mg/dL.
mL). • Bacteriostatic Water for Injec-
tion or NaCl should not be used to recon- Dosage Modification for Toxicity
stitute because of increased aggrega- Withhold or interrupt therapy; do not re-
tion. • During reconstitution, direct duce dose. Retreatment contraindicated
Sterile Water for Injection at the side of with the following toxicities: sustained
vial. Swirl contents gently to avoid foam- ventricular tachycardia, uncontrolled ar-
ing. Do not shake. rhythmias; chest pain/ECG changes con-
Rate of administration • Further di- sistent with angina or MI; cardiac tam-
lute dose in 50 mL D5W to a final concen- ponade, repetitive/refractory seizures;
tration between 0.49 and 1.1 million in- GI bleeding; bowel ischemia/perforation;
ternational units/mL (30–70 mcg/mL) renal failure requiring dialysis; coma
and infuse over 15 min. Do not use an lasting more than 48 hrs.
in-line filter. • Solution should be
warmed to room temperature before in- SIDE EFFECTS
fusion. • Monitor diligently for drop in Side effects are generally self-limited and
mean arterial B/P (sign of capillary leak resolve within 2–3 days after discontinu-
syndrome [CLS]). Continued treatment ing therapy. Frequent (89%–48%): Fever,
may result in significant hypotension chills, nausea, vomiting, hypotension,
(less than 90 mm Hg or a 20 mm Hg diarrhea, oliguria/anuria, altered mental
drop from baseline systolic pressure), status, irritability, confusion, depression,
edema, pleural effusion, altered mental sinus tachycardia, pain (abdominal,
status. chest, back), fatigue, dyspnea, pruritus.
Storage • Refrigerate vials; do not Occasional (47%–17%): Edema, ery-
freeze. • Reconstituted solution is sta- thema, rash, stomatitis, anorexia, weight
ble for 48 hrs refrigerated or at room gain, infection (UTI, injection site, cath-
temperature (refrigeration preferred). eter tip), dizziness. Rare (15%–4%): Dry

underlined – top prescribed drug


ipilimumab 619
skin, sensory disorders (vision, speech, PATIENT/FAMILY TEACHING
taste), dermatitis, headache, arthralgia, • Nausea may decrease during ther-
myalgia, weight loss, hematuria, conjunc- apy. • At home, increase fluid intake
tivitis, proteinuria. (protects against renal impairment).
ADVERSE EFFECTS/TOXIC • Do not have immunizations without
REACTIONS physician’s approval (drug lowers resis-
tance). • Avoid exposure to persons
Anemia, thrombocytopenia, leukopenia with infection. • Report fever, chills,
occur commonly. GI bleeding, pulmo- lower back pain, difficulty with urination,
nary edema occur occasionally. Capil- unusual bleeding/bruising, black tarry
lary leak syndrome (CLS) results in stools, blood in urine, petechial rash (pin-
hypotension (systolic pressure less than point red spots on skin). • Report
90 mm Hg or a 20 mm Hg drop from symptoms of depression or suicidal ide-
baseline systolic pressure), extravasa- ation immediately.
tion of plasma proteins and fluid into
extravascular space, loss of vascular I
tone. May result in cardiac arrhythmias,
angina, MI, respiratory insufficiency.
Fatal malignant hyperthermia, cardiac ipilimumab
arrest, CVA, pulmonary emboli, bowel
perforation/gangrene, severe depres- ip-i-lim-ue-mab
sion leading to suicide occur in less (Yervoy)
than 1% of pts. j BLACK BOX ALERT j Severe
and fatal immune-mediated
NURSING CONSIDERATIONS adverse reactions due to T-cell
activation and proliferation are
BASELINE ASSESSMENT capable of involving any organ
system. Specific reactions include
Pts with bacterial infection and with enterocolitis, hepatitis, dermatitis,
indwelling central lines should be neuropathy, endocrinopathy. Ma-
treated with antibiotic therapy before jority of immune-mediated reac-
treatment begins. All pts should be tions may initially manifest during
neurologically stable with a negative treatment or weeks to months after
treatment. Permanently discon-
CT scan before treatment begins. CBC, tinue treatment and initiate high-
BMP, LFT, chest X-ray should be per- dose corticosteroid therapy for
formed before therapy begins and daily severe immune-mediated adverse
thereafter. reactions. Assess all pts for signs/
symptoms of enterocolitis, hepa-
INTERVENTION/EVALUATION titis, dermatitis (including toxic
epidermal necrolysis), neuropathy,
Monitor CBC with differential, amylase, endocrinopathy, and evaluate
electrolytes, renal function, LFT, weight, clinical chemistries, including
pulse oximetry. Discontinue medication hepatic function tests and thyroid
at first sign of hypotension and hold for tests at baseline and before each
moderate to severe lethargy (physician treatment.
must decide whether therapy should uCLASSIFICATION
continue). Assess for altered mental sta-
tus (irritability, confusion, depression), PHARMACOTHERAPEUTIC: Human
weight gain/loss. Maintain strict I&O. cytotoxic T-lymphocyte antigen 4
Assess for extravascular fluid accumula- (CTLA-4)–blocking antibody. Mono-
tion (rales in lungs, edema in dependent clonal antibody. CLINICAL: Antineo-
areas). plastic.

Canadian trade name Non-Crushable Drug High Alert drug


620 ipilimumab

USES VALUES: May increase serum ALT, AST,


Treatment of unresectable or metastatic bilirubin; eosinophils.
melanoma in adults and children 12
AVAILABILITY (Rx)
yrs of age and older. Adjuvant treatment
of pts with cutaneous melanoma with Injection, Solution: 5 mg/mL (10 mL, 40
pathologic involvement of regional lymph mL vials).
nodes and who have undergone complete
ADMINISTRATION/HANDLING
resection, including total lymphadenec-
tomy. Treatment of metastatic colorectal IV
cancer (in combination with nivolumab).
b ALERT c Use sterile, nonpyrogenic,
Treatment of advanced renal cell carci-
low protein-binding in-line filter. Use
noma (in combination with nivolumab).
dedicated line only.
PRECAUTIONS Reconstitution • Calculate number of
vials needed for injection. • Inspect for
Contraindications: Hypersensitivity to
I particulate matter or discoloration. • Al-
ipilimumab. Cautions: Hepatic impair-
low vials to stand at room temperature for
ment, chronic peripheral neuropathy,
approximately 5 min. • Withdraw
thyroid/adrenal/pituitary dysfunction,
proper volume and transfer to infusion
autoimmune disorders (ulcerative coli-
bag. Dilute in NaCl or D5W with final con-
tis, Crohn’s disease, lupus, sarcoidosis).
centration ranging from 1–2 mg/
ACTION mL. • Mix diluted solution by gentle in-
version. Do not shake or agitate.
Augments T-cell activation and prolifera-
Rate of administration • Infuse over
tion. Binds to cytotoxic T-lymphocyte–as-
90 min. Flush with 0.9% NaCl or D5W at
sociated antigen 4 (CTLA-4) and blocks
end of infusion.
interaction of CTLA-4 with its ligands, al-
Storage • Solution should be translu-
lowing for enhanced T-cell activation and
cent to white or pale yellow with amor-
proliferation. Therapeutic Effect: May
phous particles. • Discard vial if cloudy
indirectly mediate T-cell immune re-
or discolored. • Refrigerate vials until
sponses against tumors.
time of use. • May store diluted solu-
PHARMACOKINETICS tion either under refrigeration or at room
temperature for no more than 24 hrs.
Metabolized in liver. Steady state reached
by third dose. Half-life: 14.7 days. INDICATIONS/ROUTES/DOSAGE
Metastatic Melanoma
LIFESPAN CONSIDERATIONS
IV: ADULTS, CHILDREN 12 YRS AND
Pregnancy/Lactation: May cause OLDER: 3 mg/kg q3wks for maximum of
fetal harm. Use effective contracep- 4 doses. Doses may be delayed due to
tion during treatment and for at least 3 toxicity, but all doses must be given
mos after discontinuation. Unknown if within 16 wks of initial dose.
distributed in breast milk. Discontinue b ALERT c Pts presenting with severe
drug or discontinue breastfeeding. immune-mediated adverse reactions must
Children: Safety and efficacy not estab- immediately discontinue drug therapy and
lished. Elderly: No age-related precau- start predniSONE 1 mg/kg/day.
tions noted.
Cutaneous Melanoma
INTERACTIONS IV: ADULTS: 10 mg/kg q3wks for 4
DRUG: May increase hepatotoxic ef- doses, then 10 mg/kg q12wks for up to 3
fect of vemurafenib. HERBAL: None yrs. If toxicity occurs, doses are omitted
significant. FOOD: None known. LAB (not delayed).

underlined – top prescribed drug


ipilimumab 621
Colorectal Cancer replacement therapy. Dermatitis including
IV: ADULTS, CHILDREN 12 YRS AND toxic epidermal necrolysis (2% of pts) may
OLDER: 1 mg/kg q3wks for up to 4 com- present with full-thickness ulceration or
bination doses, followed by nivolumab necrotic, bullous, hemorrhagic manifesta-
monotherapy. tions. Hepatotoxicity (1% of pts), defined
as LFT greater than 2.5–5 times ULN, may
Renal Cell Cancer present with right upper abdominal pain,
IV: ADULTS: 1 mg/kg q3wks for up jaundice, black/tarry stools, bruising,
to 4 combination doses, followed by dark-colored urine, nausea, vomiting. Neu-
nivolumab monotherapy. ropathy (1% of pts), including Guillain-
Dosage Modification
Barré syndrome or myasthenia gravis, may
Hold scheduled dose for moderate im- present with weakness, s­ ensory a­ lterations,
mune-mediated adverse reactions. Pts with paresthesia, paralysis. Other serious ad-
complete or partial resolution of adverse verse reactions such as pneumonitis, men-
reactions and who are receiving less than ingitis, nephritis, eosinophilia, pericarditis,
myocarditis, angiopathy, temporal arteritis, I
7.5 mg/day of predniSONE may resume
scheduled doses. Permanently discontinue vasculitis, polymyalgia rheumatica, con-
for persistent moderate adverse reactions junctivitis, blepharitis, episcleritis, scleritis,
or inability to reduce corticosteroid dose leukocytoclastic vasculitis, erythema mul-
to 7.5 mg/day, failure to complete full tiforme, psoriasis, pancreatitis, arthritis,
treatment course in 16 wks, any severe or autoimmune thyroiditis reported. Anti-
life-threatening adverse reactions. ipilimumab antibodies reported in 1.1% of
pts. All severe immune-mediated adverse
Hepatotoxicity During Treatment reactions require immediate high-dose
ALT/AST greater than 2.5 times up- corticosteroid therapy.
per limit of normal (ULN) or bilirubin
greater than 1.5–3 times ULN: With-
NURSING CONSIDERATIONS
hold treatment. ALT/AST greater than BASELINE ASSESSMENT
5 times ULN or bilirubin greater than Obtain baseline CBC, complete metabolic
3 times ULN: Permanently discontinue. profile, LFT, TSH, free T4, urine pregnancy.
Dosage in Renal/Hepatic Impairment
Screen for history of hepatic impairment,
No dose adjustment. chronic neuropathy, thyroid/adrenal/pitu-
itary dysfunction, autoimmune disorders.
SIDE EFFECTS Focused assessment relating to possible
Frequent (42%): Fatigue. Occasional
adverse reactions includes abdominal area
(32%–29%): Diarrhea, pruritus, rash, colitis.
(inspection, auscultation, percussion,
palpation, bowel pattern, symmetry),
ADVERSE EFFECTS/TOXIC skin (color, lesions, mucosal inspection,
REACTIONS edema), neurologic (mental status, gait,
Severe and fatal immune-mediated adverse numbness, tingling, pain, strength, visual
reactions have occurred. Enterocolitis acuity), hormonal glands (lymph node in-
(7% of pts) may present with fever, ileus, spection/palpation, pyrexia, goiter, palpita-
abdominal pain, GI bleeding, intestinal tions). Question possibility of pregnancy or
perforation, severe dehydrating diarrhea. plans of breastfeeding. Receive full medica-
Endocrinopathies (4% of pts), including tion history including herbal products.
hypopituitarism, adrenal insufficiency, INTERVENTION/EVALUATION
hypogonadism, hypothyroidism, may pre- Monitor vital signs, LFT, thyroid panel
sent with fatigue, headache, mental status before each dose. Continue focused as-
change, unusual bowel habits, hypoten- sessment and screen for life-threatening
sion and may require emergent hormone

Canadian trade name Non-Crushable Drug High Alert drug


622 ipratropium
immune-mediated adverse reactions. If USES
adverse reactions occur, immediately Inhalation, Nebulization: Maintenance
notify physician and initiate proper treat- treatment of bronchospasm due to COPD,
ment. Report suspected pregnancy. Obtain bronchitis, emphysema, asthma. Not indi-
CBC, blood cultures for fever, suspected cated for immediate bronchospasm relief.
infection. ECG for palpitations, chest pain, Nasal Spray: Symptomatic relief of rhi-
difficulty breathing, dizziness. If predni- norrhea associated with the common cold
SONE therapy initiated, monitor capillary and allergic/nonallergic rhinitis.
blood glucose and screen for side effects.
PATIENT/FAMILY TEACHING
PRECAUTIONS
Contraindications: History of hypersensitiv-
• Inform pt that serious and fatal adverse
ity to ipratropium, atropine. Cautions: Nar-
reactions indicate inflammation to certain
row-angle glaucoma, prostatic hypertrophy,
systems: intestines (diarrhea, dark/tarry
bladder neck obstruction, myasthenia gravis.
stools, abdominal pain), liver (yellowing
I of the skin, dark-colored urine, right up- ACTION
per quadrant pain, bruising), skin (rash,
Blocks action of acetylcholine at parasym-
mouth sores, blisters, ulcers), nerves
pathetic sites in bronchial smooth mus-
(weakness, numbness, tingling, difficulty
cle. Application to nasal mucosa inhibits
breathing, paralysis), hormonal glands
serous/seromucous gland secretions.
(headaches, weight gain, palpitations,
Therapeutic Effect: Causes broncho-
changes in mood or behavior, dizziness),
dilation, inhibits nasal s­ ecretions.
eyes (blurry vision, double vision, eye
pain/redness). • PredniSONE therapy PHARMACOKINETICS
may be started if adverse reactions oc-
Route Onset Peak Duration
cur. • May cause fetal harm, stillbirth,
premature delivery. • Blood levels will Inhalation 1–3 min 1.5–2 hrs Up to 4 hrs
Nasal 5 min 1–4 hrs 4–8 hrs
be drawn before each dose. • Report
any chest pain, palpitations, fever, swollen Minimal systemic absorption after in-
glands, stomach pain, vomiting, or any halation. Metabolized in liver (systemic
sign of adverse reactions. absorption). Primarily excreted in feces.
Half-life: 1.5–4 hrs (nasal).
LIFESPAN CONSIDERATIONS
ipratropium Pregnancy/Lactation: Unknown if dis­
ip-ra-troe-pee-um tributed in breast milk. Children/Elderly:
(Atrovent HFA, Apo-Ipratropium ) No age-related precautions noted.
Do not confuse Atrovent with INTERACTIONS
Alupent or Serevent, or ipratro-
pium with tiotropium. DRUG: Anticholinergics (e.g., aclidin-
ium, ipratropium, tiotropium, ume-
FIXED-COMBINATION(S) clidinium), medications with anticho-
Combivent, DuoNeb: ipratropium/ linergic properties may increase toxicity.
HERBAL: None significant. FOOD: None
albuterol (a bronchodilator): Aerosol:
18 mcg/90 mcg per actuation. Solu- known. LAB VALUES: None significant.
tion: 0.5 mg/2.5 mg per 3 mL. AVAILABILITY (Rx)
uCLASSIFICATION Aerosol for Oral Inhalation: (Atrovent
HFA): 17 mcg/actuation. Solution, Intra-
PHARMACOTHERAPEUTIC: Anticho-
nasal Spray: 0.03%; 0.06%. Solution for
linergic. CLINICAL: Bronchodilator.
Nebulization: 0.02% (500 mcg).

underlined – top prescribed drug


ipratropium 623

ADMINISTRATION/HANDLING 6–12 YRS: 250–500 mcg q20min for 3


Inhalation doses, then as needed. CHILDREN 5 YRS OR
• Do not shake. Prime before first use or YOUNGER: 250 mcg q20 min for 1 hr.
if not used for more than 3 days.
Rhinorrhea (Perennial Allergic/
• Instruct pt to exhale completely, place
Nonallergic Rhinitis)
mouthpiece between lips, inhale deeply
Intranasal: (0.03%): ADULTS, ELDERLY,
through mouth while fully depressing top
CHILDREN 6 YRS AND OLDER: 2 sprays per
of canister. Hold breath as long as possible
nostril 2–3 times/day.
before exhaling slowly. • Allow at least 1
minute between inhalations. • Rinse Rhinorrhea (Common Cold)
mouth with water immediately after inha- Intranasal: (0.06%): ADULTS, ELDERLY,
lation (prevents mouth/throat dryness). CHILDREN 12 YRS AND OLDER: 2 sprays per
nostril 3–4 times/day for up to 4 days.
Nebulization
CHILDREN 5–11 YRS: 2 sprays per nostril
• May be administered with or without
3 times/day for up to 4 days. I
dilution in 0.9% NaCl. • Stable for 1 hr
when mixed with albuterol. • Give over Rhinorrhea (Seasonal Allergy)
5–15 min. Intranasal: (0.06%): ADULTS, ELDERLY,
CHILDREN 5 YRS AND OLDER: 2 sprays per
Nasal
nostril 4 times/day for up to 3 wks.
• Store at room temperature. • Initial
pump priming requires 7 actuations of Dosage in Renal/Hepatic Impairment
pump. • If used regularly as recom- No dose adjustment.
mended, no further priming is required.
If not used for more than 4 hrs, pump SIDE EFFECTS
will require 2 actuations, or if not used Frequent: Inhalation (6%–3%): Cough,
for more than 7 days, the pump will re- dry mouth, headache, nausea. Nasal: Dry
quire 7 actuations to reprime. nose/mouth, headache, nasal irritation.
Occasional: Inhalation (2%): Dizziness,
INDICATIONS/ROUTES/DOSAGE transient increased bronchospasm. Rare
Bronchodilator for COPD (less than 1%): Inhalation: Hypotension,
Inhalation: ADULTS, ELDERLY, CHILDREN insomnia, metallic/unpleasant taste, palpi-
2 inhalations 4 times/
OLDER THAN 12 YRS: tations, urinary retention. Nasal: Diarrhea,
day. Maximum: 12 inhalations per 24 hrs. constipation, dry throat, abdominal pain,
Nebulization: ADULTS, ELDERLY, CHIL- nasal congestion.
DREN OLDER THAN 12 YRS: 500 mcg
(1 unit dose vial) 3–4 times/day (doses ADVERSE EFFECTS/
6–8 hrs apart). TOXIC REACTIONS
Worsening of angle-closure glaucoma,
Asthma Exacerbation
acute eye pain, hypotension occur rarely.
Note: Should be given in combination
with a short-acting beta-adrenergic agonist.
Inhalation: ADULTS, ELDERLY, CHILDREN
NURSING CONSIDERATIONS
OLDER THAN 12 YRS: 8 inhalations q20min BASELINE ASSESSMENT
as needed for up to 3 hrs. CHILDREN 6–12 Auscultate lung sounds. Question history
YRS: 4–8 inhalations q20min as needed
of glaucoma, urinary retention, myasthe-
for up to 3 hrs. CHILDREN 5 YRS OR nia gravis.
YOUNGER: 2 inhalations q20 min for 1 hr.
Nebulization: ADULTS, ELDERLY, CHIL- INTERVENTION/EVALUATION
DREN OLDER THAN 12 YRS:500 mcg q20min Monitor rate, depth, rhythm, type of
for 3 doses, then as needed. CHILDREN respiration; quality, rate of pulse. Assess

Canadian trade name Non-Crushable Drug High Alert drug


624 irbesartan
lung sounds for rhonchi, wheezing, rales. PRECAUTIONS
Monitor ABGs. Observe for retractions
(clavicular, sternal, intercostal), hand Contraindications: Hypersensitivity to
tremor. Evaluate for clinical improvement irbesartan. Concomitant use with aliski-
(quieter, slower respirations, relaxed fa- ren in pts with diabetes. Cautions: Renal
cial expression, cessation of retractions). impairment, unstented unilateral or bi-
Monitor for improvement of rhinorrhea. lateral renal artery stenosis, dehydration,
HF, idiopathic or hereditary angioedema
PATIENT/ FAMILY TEACHING or angioedema associated with ACE in-
• Increase fluid intake (decreases lung hibitor therapy.
secretion viscosity). • Do not take more
than 2 inhalations at any one time (exces- ACTION
sive use may produce paradoxical bron- Blocks vasoconstriction, aldosterone-
choconstriction, decreased bronchodilat- secreting effects of angiotensin II, inhibit-
ing effect). • Rinsing mouth with water ing binding of angiotensin II to AT1 re-
I immediately after inhalation may prevent ceptors. Therapeutic Effect: Produces
mouth and throat dryness. • Avoid ex- vasodilation, decreases peripheral resis-
cessive use of caffeine derivatives (choco- tance, decreases B/P.
late, coffee, tea, cola, cocoa).
PHARMACOKINETICS
Route Onset Peak Duration
PO — 1–2 hrs Greater than 24 hrs
irbesartan Rapidly, completely absorbed after PO
ir-be-sar-tan administration. Protein binding: 90%.
(Avapro) Metabolized in liver. Excreted in feces
(80%), urine (20%). Not removed by
j BLACK BOX ALERT jMay cause hemodialysis. Half-life: 11–15 hrs.
fetal injury, mortality if used during
second or third trimester of pregnan-
cy. Discontinue as soon as possible LIFESPAN CONSIDERATIONS
once pregnancy is detected. Pregnancy/Lactation: Unknown if
Do not confuse Avapro with distributed in breast milk. May cause
Anaprox. fetal or neonatal morbidity or mortality.
Children: Safety and efficacy not estab-
FIXED-COMBINATION(S) lished. Elderly: No age-related precau-
Avalide: irbesartan/hydroCHLORO- tions noted.
thiazide (a diuretic): 150 mg/12.5 mg,
300 mg/12.5 mg, 300 mg/25 mg. INTERACTIONS
DRUG: Aliskiren may increase hyper-
uCLASSIFICATION
kalemic effect. May increase adverse of
PHARMACOTHERAPEUTIC: Angio- ACE inhibitors (e.g., benazepril,
tensin II receptor antagonist. CLINI- lisinopril). NSAIDs (e.g., ibuprofen,
CAL: Antihypertensive. ketorolac, naproxen) may decrease
antihypertensive effect. HERBAL: Herb-
als with hypertensive properties
USES (e.g., licorice, yohimbe) or hypo-
Treatment of hypertension alone or in tensive properties (e.g., garlic, gin-
combination with other antihyperten- ger, ginkgo biloba) may alter effects.
sives. Treatment of diabetic nephropathy FOOD: None known. LAB VALUES: May
in pts with type 2 diabetes. OFF-LABEL: slightly increase serum BUN, creatinine.
Reduce proteinuria in children with May decrease Hgb.
chronic kidney disease.
underlined – top prescribed drug
irinotecan 625

AVAILABILITY (Rx) PATIENT/ FAMILY TEACHING


Tablets: 75 mg, 150 mg, 300 mg. • May cause fetal or neonatal morbidity
or mortality. • Avoid tasks that require
ADMINISTRATION/HANDLING alertness, motor skills until response to
PO drug is established (possible dizziness ef-
• Give without regard to food. fect); ensure that appropriate birth control
measures are in place. • Report any sign
INDICATIONS/ROUTES/DOSAGE of infection (sore throat, fever). • Avoid
Hypertension exercising during hot weather (risk of de-
PO: ADULTS, ELDERLY, CHILDREN 13 YRS hydration, hypotension).
AND OLDER: Initially, 75–150 mg/day.
May increase to 300 mg/day. CHILDREN
6–12 YRS: Initially, 75 mg/day. May in- irinotecan
crease to 150 mg/day.
eye-ri-noe-tee-kan
Diabetic Nephropathy (Camptosar, Onivyde) I
PO: ADULTS, ELDERLY: 300 mg once j BLACK BOX ALERT j (Campto-
daily. sar, Onivyde): Can induce both early
and late forms of severe diarrhea.
Dosage in Renal/Hepatic Impairment Early diarrhea (during or shortly
No dose adjustment. after administration) accompanied
by salivation, rhinitis, lacrimation,
SIDE EFFECTS diaphoresis, flushing. Late diarrhea
(occurring more than 24 hrs after
Occasional (9%–3%): Upper respiratory administration) can be prolonged
tract infection, fatigue, diarrhea, cough. and life-threatening. (Camptosar):
Rare (2%–1%): Heartburn, dizziness, May produce severe, profound my-
elosuppression. Administer under
headache, nausea, rash. supervision of experienced cancer
chemotherapy physician.  (Onivyde):
ADVERSE EFFECTS/TOXIC Severe, life-threatening, or fatal
REACTIONS neutropenic fever/sepsis occurred.
Overdose may manifest as hypotension, Withhold for ANC below 1,500 cells/
mm3 or neutropenic fever. Monitor
syncope, tachycardia. Bradycardia oc- blood cell counts.
curs less often.
uCLASSIFICATION
NURSING CONSIDERATIONS PHARMACOTHERAPEUTIC: Topoi-
BASELINE ASSESSMENT
somerase inhibitor. CLINICAL: Anti-
neoplastic.
Obtain B/P, apical pulse immediately
before each dose in addition to regular
monitoring (be alert to fluctuations). USES
Question possibility of pregnancy. As- Camptosar: Treatment of metastatic carci-
sess medication history (esp. diuretic noma of colon or rectum. Onivyde: Treat-
therapy). ment of metastatic adenocarcinoma of the
INTERVENTION/EVALUATION pancreas (in combination with 5-fluoroura-
Maintain hydration (offer fluids fre- cil and leucovorin) after ­disease progres-
quently). Assess for evidence of upper sion following gemcitabine-based therapy.
OFF-LABEL: Non–small-cell lung cancer;
respiratory infection. Assist with ambu-
lation if dizziness occurs. Monitor elec- small-cell lung cancer; CNS tumor; cervi-
trolytes, renal function, urinalysis, B/P, cal, gastric, pancreatic, ovarian, esophageal
pulse. Assess for hypotension. cancer; Ewing’s sarcoma; brain tumor.

Canadian trade name Non-Crushable Drug High Alert drug


626 irinotecan

PRECAUTIONS AVAILABILITY (Rx)


Contraindications: Hypersensitivity to Injection Solution: (Conventional): 20
irinotecan. Cautions: Pt previously re- mg/mL (2 mL, 5 mL, 15 mL, 25 mL).
ceiving pelvic, abdominal irradiation (in- (Liposomal): 43 mg/10 mL.
creased risk of myelosuppression), pts
older than 65 yrs, hepatic dysfunction, ADMINISTRATION/HANDLING
hyperbilirubinemia, renal impairment, IV
preexisting pulmonary disease.
Camptosar
ACTION Reconstitution • Dilute in D5W (pre-
Binds reversibly with topoisomerase I, an ferred) or 0.9% NaCl to concentration of
enzyme that relieves torsional strain in 0.12–2.8 mg/mL.
Rate of administration • Administer
DNA by inducing reversible single-strand
breaks. Prevents religation of these sin- all doses as IV infusion over 30–90
gle-stranded breaks, resulting in damage min. • Assess for extravasation (flush
I site with Sterile Water for Injection, apply
to double-strand DNA, cell death. Thera-
peutic Effect: Produces cytotoxic effect ice if extravasation occurs).
Storage • Store vials at room tempera-
on cancer cells.
ture, protect from light. • Solution diluted
PHARMACOKINETICS with D5W is stable for 24 hrs at room tem-
perature or 48 hrs if refrigerated. • Solu-
Metabolized in liver. Protein binding: tion diluted with 0.9% NaCl is stable for 24
95% (metabolite). Excreted in urine hrs at room temperature. • Do not refrig-
and eliminated by biliary route. Half- erate solution if diluted with 0.9% NaCl.
life: 6–12 hrs; metabolite, 10–20 hrs.
Onivyde
LIFESPAN CONSIDERATIONS Reconstitution • Withdraw dose
Pregnancy/Lactation: May cause fetal from vial and dilute with 500 mL D5W or
harm. Unknown if distributed in breast 0.9% NaCl. Mix gently.
milk. Breastfeeding not recommended. Rate of administration • Infuse over
Children: Safety and efficacy not estab- 90 min.
lished. Elderly: Risk of diarrhea signifi- Storage • Refrigerate vials; do not
cantly increased. freeze. • Protect from light. • Stable
for 4 hrs at room temperature or 24 hrs
INTERACTIONS refrigerated.
DRUG: Strong CYP3A4 inducers IV INCOMPATIBILITIES
(e.g., carBAMazepine, phenytoin,
Gemcitabine (Gemzar).
rifAMPin) may decrease concentration/
effect. Strong CYP3A4 inhibitors (e.g., INDICATIONS/ROUTES/DOSAGE
clarithromycin, ketoconazole, rito- Note: Genotyping of UGTIAI available. Pts
navir) may increase concentration/effect. who are homozygous for the UGTIAI*28
May decrease the therapeutic effect of BCG allele are at increased risk for neutrope-
(intravesical), vaccines (live). May in- nia. Decreased dose is recommended.
crease adverse effects of vaccines (live).
UGT1A1 inhibitors (e.g., erlotinib, Carcinoma of the Colon, Rectum
nilotinib) may increase concentration/ (Camptosar)
effect. HERBAL: St. John’s wort may de- IV: (Single-Agent Therapy): ADULTS,
crease concentration/effect. FOOD: None ELDERLY: (WEEKLY REGIMEN): Initially, 125
known. LAB VALUES: May increase serum mg/m2 once wkly for 4 wks, followed by
alkaline phosphatase, AST. May decrease a rest period of 2 wks. Additional courses
Hgb, leukocytes, platelets. may be repeated q6wks. Dosage may be
underlined – top prescribed drug
isavuconazonium 627
adjusted in 25–50 mg/m2
increments/ dose. Premedicate with antiemetics on
decrements to as high as 150 mg/m2 day of treatment, starting at least 30 min
or as low as 50 mg/m2. (3-WEEK REGI- before administration. Inform pt of pos-
MEN): 350 mg/m2 q3wks. Dosage may sibility of alopecia.
be adjusted to as low as 200 mg/m2 in
INTERVENTION/EVALUATION
decrements of 25–50 mg/m2.
(In Combination with Leucovorin Monitor daily pattern of bowel activ-
and 5-Fluorouracil): REGIMEN 1: 125 ity, stool consistency. Monitor hydration
mg/m2 on days 1, 8, 15, 22. Dose may status, I&O, electrolytes, CBC, renal func-
be adjusted to 100 mg/m2, then 75 mg/ tion, LFT. Monitor infusion site for signs
m2, then decrements of approximately of inflammation. Assess skin for rash.
20%. REGIMEN 2: 180 mg/m2 on days 1, PATIENT/ FAMILY TEACHING
15, 29. Dose may be adjusted to 150 mg/
m2, then 120 mg/m2, then decrements of • Report diarrhea, vomiting, fever, light-
approximately 20%. headedness, dizziness. • Do not have
immunizations without physician’s ap- I
Pancreatic Cancer (Onivyde) proval (drug lowers resistance). • Avoid
IV Infusion: ADULTS, ELDERLY: 70 mg/ contact with those who have recently re-
m2 once q2wks (in combination with ceived live virus vaccine. • Avoid
leucovorin and 5-fluorouracil). crowds, those with infections.

Dosage in Renal Impairment


No dose adjustment.
isavuconazonium
Dosage in Hepatic Impairment
eye-sa-vue-kon-a-zoe-nee-um
Serum Bilirubin Dose (Cresemba)
Greater than ULN to 2 Reduce dose one
mg/dL: level uCLASSIFICATION
Greater than 2 mg/dL: Not recommended
PHARMACOTHERAPEUTIC: Azole
antifungal derivative. CLINICAL: An-
SIDE EFFECTS tifungal.
Expected (64%–32%): Nausea, alope-
cia, vomiting, diarrhea. Frequent (29%– USES
22%): Constipation, fatigue, fever, asthenia,
skeletal pain, abdominal pain, dyspnea. Treatment of invasive aspergillosis and inva-
Occasional (19%–16%): Anorexia, head- sive mucormycosis in pts 18 yrs and older.
ache, stomatitis, rash. PRECAUTIONS
ADVERSE EFFECTS/TOXIC Contraindications: Hypersensitivity to
REACTIONS isavuconazonium or isavuconazole, con-
Hematologic toxicity characterized by comitant use of strong CYP3A inhibitors
anemia, leukopenia, thrombocytopenia, (e.g., ketoconazole, high-dose ritonavir),
and neutropenia, sepsis occur frequently. strong CYP3A inducers (e.g., carBAMaze-
Camptosar may cause severe/fatal inter- pine, rifAMPin, St. John’s wort), history
stitial lung disease. of short QT syndrome. Cautions: Renal/
hepatic impairment, hypersensitivity to
NURSING CONSIDERATIONS other azoles. Pts at risk for acute pan-
creatitis; concomitant use of nephrotoxic
BASELINE ASSESSMENT medications; pts at risk for hypokalemia,
Offer emotional support. Assess hydra- hypomagnesemia. Concomitant use of
tion status, electrolytes, CBC before each medications that prolong QT interval.
Canadian trade name Non-Crushable Drug High Alert drug
628 isavuconazonium

ACTION ADMINISTRATION/HANDLING
Isavuconazonium is the prodrug of IV
isavuconazole. Interferes with fungal
cytochrome activity, decreasing ergos- Reconstitution • Reconstitute vial
terol synthesis, inhibiting fungal cell with 5 mL Sterile Water for Injec-
membrane formation. Therapeutic tion. • Gently shake until completely
Effect: Damages fungal cell wall mem- dissolved. • Visually inspect for partic-
brane. ulate matter or discoloration. Solution
may contain visible translucent to white
PHARMACOKINETICS particles. • Inject reconstituted solu-
Widely distributed. Metabolized in liver. tion into 250 mL 0.9% NaCl or 5% Dex-
Protein binding: greater than 99%. Peak trose injection. • Gently invert bag to
plasma concentration: 2–3 hrs. Excreted mix. Do not shake or agitate. Do not use
in feces (46%), urine (46%). Half- pneumatic transport system. • Diluted
life: 130 hrs. solution may also contain visible translu-
I cent to white particles (which will be re-
LIFESPAN CONSIDERATIONS moved by in-line filter).
Pregnancy/Lactation: May cause Administration • Do not give as IV
fetal harm. Avoid pregnancy. Avoid push or bolus. Flush IV line with 0.9%
breastfeeding while taking Cresemba. NaCl or 5% Dextrose injection prior to
Children: Safety and efficacy not es- and after infusion.
tablished. Elderly: No age-related pre- Rate of administration • Infuse over
cautions noted. 60 min (minimum) using 0.2- to
1.2-­micron in-line filter.
INTERACTIONS Storage • Diluted solution may be
DRUG: Strong CYP3A4 inhibitors stored at room temperature up to 6 hrs or
(e.g., clarithromycin, ketocon- refrigerated up to 24 hrs. • Do not freeze.
azole, ritonavir) may increase con-
centration/effect. Strong CYP3A4 PO
inducers (e.g., carBAMazepine, • Give without regard to food. • Do
rifAMPin) may decrease concentra- not cut, crush, divide, or open capsules.
tion/effect. May increase concentration/ INDICATIONS/ROUTES/DOSAGE
effects of cycloSPORINE, digoxin,
eplerenone, estrogen, everolimus, Note: 372 mg is equivalent to 200 mg
midazolam, mycophenolate siro- isavuconazole. Duration of therapy: mini-
limus, tacrolimus. May decrease mum of 6–12 wks.
therapeutic effect of Saccharomyces Invasive Aspergillosis, Invasive
boulardii. HERBAL: St. John’s wort Mucormycosis
may decrease concentration/effect. IV: ADULTS, ELDERLY: Loading dose:
FOOD: None known. LAB VALUES: May 372 mg q8h for 6 doses (48 hrs). Main-
increase serum alkaline phosphatase, tenance: 372 mg once daily. Start main-
ALT, AST, bilirubin. May decrease serum tenance dose 12–24 hrs after last loading
potassium, magnesium. dose. PO: ADULTS, ELDERLY: Loading
AVAILABILITY (Rx) dose: 372 mg (2 capsules) q8h for 6
doses (48 hrs). Maintenance: 372 mg
372 mg/vial (equiva-
Injection Powder: (2 capsules) once daily. Start maintenance
lent to 200 mg isavuconazole). Cap- dose 12–24 hrs after last loading dose.
sules: 186 mg (equivalent to 100 mg
isavuconazole). Dosage in Renal Impairment
No dose adjustment.

underlined – top prescribed drug


isoniazid 629
Dosage in Hepatic Impairment reproductive potential should use effec-
Mild to moderate impairment: No tive contraception. Immediately report
dose adjustment. Severe impairment: suspected pregnancy. • Do not take
Not specified; use caution. herbal products such as St. John’s
wort. • Report liver problems such as
SIDE EFFECTS upper abdominal pain, bleeding, dark or
Frequent (28%–17%): Nausea, vomiting, amber-colored urine, nausea, vomiting,
diarrhea, abdominal pain, headache, dys- or yellowing of the skin or eyes. • Re-
pnea. Occasional (15%–6%): Peripheral port decreased urinary output, extremity
edema, constipation, fatigue, insomnia, swelling, dark-colored urine; skin
back pain, delirium, agitation, confusion, changes such as rash, skin bubbling, or
disorientation, chest pain, rash, pruritus, sloughing.
hypotension, anxiety, dyspepsia, injection
site reaction, decreased appetite.
ADVERSE EFFECTS/TOXIC isoniazid I
REACTIONS
Severe hepatic injury including cholesta- eye-soe-nye-a-zid
sis, hepatitis, hepatic failure reported in (Isotamine )
pts with underlying medical conditions j BLACK BOX ALERT jSevere,
(e.g., hematologic malignancies). Infu- potentially fatal hepatitis may occur.
sion-related reactions including chills,
dizziness, dyspnea, hypoesthesia, hypo- FIXED-COMBINATION(S)
tension, paresthesia may occur. Acute Rifamate: isoniazid/rifAMPin (antitu-
respiratory failure, renal failure, Stevens- bercular): 150 mg/300 mg.
Johnson syndrome, serious hypersensi- Rifater: isoniazid/pyrazinamide/ri-
tivity reaction (including anaphylaxis) fAMPin (antitubercular): 50 mg/300
were reported. mg/120 mg.
NURSING CONSIDERATIONS uCLASSIFICATION
BASELINE ASSESSMENT PHARMACOTHERAPEUTIC: Isonico-
Obtain baseline LFT. Confirm negative tinic acid derivative. CLINICAL: An-
pregnancy test before initiating treat- titubercular.
ment. Specimens for fungal culture, his-
topathology should be obtained prior to
initiating therapy. Receive full medication USES
history and screen for interactions/con- Treatment of susceptible active tuberculo-
traindications. Question history of hyper- sis due to Mycobacterium tuberculosis.
sensitivity reaction, hepatic impairment. Treatment of latent tuberculosis caused
by Mycobacterium tuberculosis.
INTERVENTION/EVALUATION
Monitor BMP, LFT periodically. Monitor PRECAUTIONS
for infusion-related reactions, hypersen- Contraindications:Hypersensitivity to
sitivity reactions, anaphylaxis. Monitor isoniazid (including drug-induced
I&O. Report worsening of hepatic/renal hepatitis), acute hepatic disease, he-
function. patic injury or severe adverse reac-
PATIENT/FAMILY TEACHING tions with previous isoniazid therapy.
Cautions: Chronic hepatic disease,
• Swallow capsule whole; do not chew, alcoholism, severe renal impairment.
crush, cut, or open capsules. • Treat- Pregnancy, pts at risk for peripheral
ment may cause fetal harm. Females of

Canadian trade name Non-Crushable Drug High Alert drug


630 isoniazid
neuropathy, HIV infection, history of AVAILABILITY (Rx)
hypersensitivity reactions to latent TB
­ Solution, Injection: 100 mg/mL. Syrup, Oral:
infection medications. 50 mg/5 mL. Tablets: 100 mg, 300 mg.
ACTION ADMINISTRATION/HANDLING
Inhibits mycolic acid synthesis. Causes PO
disruption of bacterial cell wall, loss • Give 1 hr before or 2 hrs following
of acid-fast properties in susceptible meals (may give with food to decrease GI
mycobacteria. Therapeutic Effect: upset, but will delay absorption). • Ad-
Bactericidal against actively growing in- minister at least 1 hr before antacids,
tracellular, extracellular susceptible my- esp. those containing aluminum.
cobacteria.
INDICATIONS/ROUTES/DOSAGE
PHARMACOKINETICS Active Tuberculosis (in Combination with
Note: Isoniazid is metabolized by acety- One or More Antituberculars)
I lation. The rate of acetylation is geneti- IM/PO: ADULTS, ELDERLY, CHILDREN
cally determined (e.g., 50% of black WEIGHING 40 KG OR MORE: 5 mg/kg once
and Caucasian pts are slow inactivators; daily. Usual dose: 300 mg. CHILDREN
Eskimo and Asian pts are rapid inacti- WEIGHING LESS THAN 40 KG: 10–15 mg/
vators. Slower inactivation may lead to kg once daily. Maximum: 300 mg.
higher blood levels and increased ad- Note: Give isoniazid with rifAMPin, pyra-
verse effects. zinamide, and with or without ethambu-
Readily absorbed from GI tract. Protein tol for 8 wks, then give with rifAMPin for
binding: 10%–15%. Widely distributed 18 wks.
(including to CSF). Metabolized in liver.
Primarily excreted in urine. Removed by Latent Tuberculosis
hemodialysis. Half-life: (Fast acetyl- Note: Give for 9 mos.
ators): 30–100 min; (slow acetylators): IM/PO: ADULTS, ELDERLY, CHILDREN 12
2–5 hrs. YRS AND OLDER: 5 mg/kg once daily
(Maximum: 300 mg) or 15 mg/kg
LIFESPAN CONSIDERATIONS twice wkly (Maximum: 900 mg).
CHILDREN LESS THAN 12 YRS: 10–20 mg/
Pregnancy/Lactation: Prophylaxis
kg/day as a single daily dose. Maxi-
usually postponed until after delivery.
mum: 300 mg/day or 20–40 mg/kg 2
Crosses placenta. Distributed in breast
times/wk. Maximum: 900 mg/dose.
milk. Children: No age-related precau-
tions noted. Elderly: More susceptible Dosage in Renal Impairment
to developing hepatitis. No dose adjustment.
INTERACTIONS Dosage in Hepatic Impairment
DRUG: May increase concentration/ Use caution. Contraindicated with acute
effect of carBAMazepine, fosphenyt- hepatic disease.
oin, lomitapide, phenytoin. Hepato- SIDE EFFECTS
toxic medications (e.g., acetamino-
phen, rifAMPin) may increase risk of Frequent: Nausea, vomiting, diarrhea,
hepatotoxicity. May decrease ketocon- abdominal pain. Rare: Pain at injection
azole concentration. HERBAL: None site, hypersensitivity reaction.
significant. FOOD: Foods containing ADVERSE EFFECTS/TOXIC
tyramine may cause hypertensive cri- REACTIONS
sis. LAB VALUES: May increase serum
Neurotoxicity (ataxia, paresthesia), optic
bilirubin, ALT, AST.
neuritis, hepatotoxicity occur rarely.

underlined – top prescribed drug


isosorbide dinitrate 631

NURSING CONSIDERATIONS isosorbide


BASELINE ASSESSMENT
Question for history of hypersensitiv-
­mononitrate
ity reactions, hepatic injury or disease, (Apo-ISMN , Imdur )
sensitivity to nicotinic acid or chemically Do not confuse Imdur with Imu-
related medications. Ensure collection of ran, Inderal, or K-Dur, Isordil
specimens for culture, sensitivity. Evalu- with Inderal, Isuprel, or Plendil.
ate initial LFT.
INTERVENTION/EVALUATION
FIXED-COMBINATION(S)
BiDil: isosorbide dinitrate/hydrALA-
Monitor LFT, assess for hepatitis: an-
ZINE (a vasodilator): 20 mg/37.5 mg.
orexia, nausea, vomiting, weakness,
fatigue, dark urine, jaundice (withhold uCLASSIFICATION
concurrent INH therapy and inform
PHARMACOTHERAPEUTIC: Nitrate.
physician promptly). Assess for pares- I
CLINICAL: Antianginal.
thesia of extremities (pts esp. at risk
for neuropathy may be given pyridoxine
prophylactically: malnourished, elderly, USES
diabetics, pts with chronic hepatic dis- Dinitrate: Prevention of angina pectoris
ease [including alcoholics]). Be alert due to coronary artery disease. Mono-
for fever, skin eruptions (hypersensitivity nitrate: Treatment (immediate-release
reaction). only) and prevention of angina pecto-
PATIENT/FAMILY TEACHING ris due to coronary artery disease.
• Do not skip doses; continue to take PRECAUTIONS
isoniazid for full length of therapy (6–24 Contraindications: Hypersensitivity to
mos). • Take preferably 1 hr before or nitrates, concurrent use of sildenafil,
2 hrs following meals (with food if GI tadalafil, vardenafil, or riociguat. Cau-
upset). • Avoid alcohol during treat- tions: Inferior wall MI, head trauma,
ment. • Do not take any other medica- increased intracranial pressure (ICP),
tions, including antacids, without con- orthostatic hypotension, blood volume
sulting physician. • Must take isoniazid depletion from diuretic therapy, systolic
at least 1 hr before antacid. • Avoid B/P less than 90 mm Hg, hypertrophic
tuna, sauerkraut, aged cheeses, smoked cardiomyopathy, alcohol consumption.
fish (consult list of tyramine-containing
foods), which may cause hypertensive ACTION
reaction (red/itching skin, palpitations, Activates intracellular cyclic guanosine mo-
light-headedness, hot or clammy feeling, nophosphate. Therapeutic Effect: Re-
headache). • Report any new symp- laxes vascular smooth muscle of arterial,
tom, immediately for vision difficulties, venous vasculature. Decreases preload,
nausea/vomiting, dark urine, yellowing afterload, cardiac oxygen demand.
of skin/eyes (jaundice), fatigue, pares-
thesia of extremities. PHARMACOKINETICS
Route Onset Peak Duration
Dinitrate
Sublingual 3 min N/A 1–2 hrs
isosorbide dinitrate PO 45–60 min N/A up to 8
hrs
eye-soe-sor-bide Mononitrate
PO (extended- 30–60 min N/A 12–24
(ISDN , Dilatrate-SR, Isordil) release) hrs

Canadian trade name Non-Crushable Drug High Alert drug


632 isosorbide dinitrate

Dinitrate poorly absorbed and metabo- Initially, 5–20


Release): ADULTS, ELDERLY:
lized in liver to its active metabolite iso- mg 2–3 times/day. Maintenance: 10–40
sorbide mononitrate. Mononitrate well mg (or between 5–80 mg) 2–3 times/day.
absorbed after PO administration. Pri- (Sustained-Release): ADULTS, EL-
marily excreted in urine. Half-life: Di- DERLY: 40 mg 1–2 times/day. A nitrate-
nitrate, 1–4 hrs; mononitrate, 4 hrs. free interval of greater than 18 hrs is
recommended.  Maximum: 160 mg/day.
LIFESPAN CONSIDERATIONS PO: (Isosorbide Mononitrate) (Imme-
Pregnancy/Lactation: Unknown if drug diate-Release): ADULTS, ELDERLY: 20 mg
crosses placenta or is distributed in breast twice daily given 7 hrs apart to decrease toler-
milk. Children: Safety and efficacy not es- ance development. In pts with small stature,
tablished. Elderly: May be more sensitive may start at 5 mg twice daily and titrate to
to hypotensive effects. Age-related renal im- at least 10 mg twice daily in first 2–3 days
pairment may require dosage adjustment. of therapy. (Sustained-Release): Initially,
30–60 mg/day in morning as a single dose.
I INTERACTIONS May increase dose at 3-day intervals to 120
DRUG: Alcohol, riociguat, sildenafil, mg once daily. Maximum daily single
tadalafil, vardenafil may potentiate dose: 240 mg.
hypotensive effects (concurrent use of
Dosage in Renal/Hepatic Impairment
these agents is contraindicated). Strong
No dose adjustment.
CYP3A4 inhibitors (e.g., clarithromy-
cin, ketoconazole, ritonavir) may in- SIDE EFFECTS
crease concentration/effect. HERBAL: St. Frequent: Headache (may be severe) oc-
John’s wort may decrease concentra- curs mostly in early therapy, diminishes
tion/effect. FOOD: None known. LAB VAL- rapidly in intensity, usually disappears
UES: May increase urine catecholamine,
during continued treatment. Sublingual:
urine vanillylmandelic acid levels. Burning, tingling at oral point of dissolu-
AVAILABILITY (RX) tion. Occasional: Transient flushing of
face/neck, dizziness, weakness, orthostatic
Dinitrate
hypotension, nausea, vomiting, restless-
Tablets: 5 mg, 10 mg, 20 mg, 30 mg, 40 mg.
ness. GI upset, blurred vision, dry mouth.
Capsules, Extended-Release: 40 mg.
Tablets, Extended-Release: 40 mg. ADVERSE EFFECTS/TOXIC
REACTIONS
Mononitrate Discontinue if blurred vision occurs. Se-
Tablets: 10 mg, 20 mg. vere orthostatic hypotension manifested by
Tablets, Extended-Release: 30 mg, syncope, pulselessness, cold/clammy skin,
60 mg, 120 mg. diaphoresis has been reported. Toler-
ance may occur with repeated, prolonged
ADMINISTRATION/HANDLING therapy, but may not occur with extended-­
PO release form. Minor tolerance with in-
• Best if taken on an empty stomach. termittent use of sublingual tablets. High
• Do not administer around the clock. dosage tends to produce severe headache.
• Oral tablets may be crushed. • Do
not crush/break sustained-, extended- NURSING CONSIDERATIONS
release form. BASELINE ASSESSMENT
INDICATIONS/ROUTES/DOSAGE Record onset, type (sharp, dull, squeez-
Angina ing), radiation, location, intensity,
Note: Dinitrate used only for prevention. ­duration of anginal pain; precipitating fac-
PO: (Isosorbide Dinitrate) (Immediate- tors (exertion, emotional stress). If head-

underlined – top prescribed drug


itraconazole 633
ache occurs during management therapy, voriconazole, or Sporanox with
administer medication with meals. Suprax or Topamax.
INTERVENTION/EVALUATION uCLASSIFICATION
Assist with ambulation if light-headed- PHARMACOTHERAPEUTIC: Imida-
ness, dizziness occurs. Assess for facial/ zole/triazole type antifungal. CLINI-
neck flushing. Monitor number of angi- CAL: Antifungal.
nal episodes, orthostatic B/P.
PATIENT/FAMILY TEACHING USES
• Do not chew, crush, dissolve, or divide Oral capsules: Treatment of aspergil-
sublingual, extended-release, sustained- losis, blastomycosis, esophageal and
release forms. • Take sublingual tablets oropharyngeal candidiasis, empiric
while sitting down. • Go from lying to treatment in febrile neutropenia, histo-
standing slowly (prevents dizziness ef- plasmosis, onychomycosis. Oral solu-
fect). • Take oral form on empty stom- tion: Treatment of oral and esophageal I
ach (however, if headache occurs during candidiasis. Oral tablet: Treatment of
management therapy, take medication onychomycosis of toenail.
with meals). • Dissolve sublingual tab-
let under tongue; do not swallow. PRECAUTIONS
• Avoid alcohol (intensifies hypotensive Contraindications: Hypersensitivity to
effect). • If alcohol is ingested soon af- itraconazole, other azoles. Treatment of
ter taking nitrates, possible acute hypo- onychomycosis in pts with evidence of ven-
tensive episode (marked drop in B/P, tricular dysfunction (e.g., HF or history of
vertigo, pallor) may occur. • Report HF); concurrent use of dofetilide, droned-
signs/symptoms of hypotension, angina. arone, eplerenone, ergot derivatives, felo-
dipine, irinotecan, lovastatin, lurasidone,
methadone, midazolam (oral), pimozide,
itraconazole ranolazine, simvastatin, ticagrelor, tri-
azolam, quiNIDine; concurrent use with
it-ra-kon-a-zole colchicine, fesoterodine, solifenacin in
(Sporanox, Tolsura) pts with renal/hepatic impairment; treat-
j BLACK BOX ALERT jSerious ment of onychomycosis in women who
cardiovascular events, includ- are pregnant or are intending to become
ing HF, ventricular tachycardia, pregnant. Cautions: Preexisting hepatic
torsades de pointes, death, have
occurred due to concurrent use impairment (not recommended in pts
with colchicine (pts with renal/ with active hepatic disease, elevated LFTs),
hepatic impairment), dofetilide, renal impairment, pts with risk factors for
dronedarone, eplerenone, ergot HF (e.g., COPD, myocardial ischemia).
alkaloids, felodipine, fesoterodine,
irinotecan, ivabradine, levometha- ACTION
dyl, lovastatin, lurasidone, metha-
done, midazolam (oral), pimozide, Inhibits synthesis of ergosterol (vital com-
quiNIDine, ranolazine, simvastatin, ponent of fungal cell formation). Thera-
solifenacin, ticagrelor, or triazolam. peutic Effect: Damages fungal cell mem-
Negative inotropic effects observed brane, altering its function. Fungistatic.
following IV administration.
Contraindicated for treatment of PHARMACOKINETICS
onychomycosis in pts with HF,
ventricular dysfunction. Moderately absorbed from GI tract. Ab-
Do not confuse itraconazole sorption is increased when taken with
with fluconazole, ketoconazole, food. Protein binding: 99%. Widely dis-
miconazole, posaconazole, tributed, primarily in fatty tissue, liver,

Canadian trade name Non-Crushable Drug High Alert drug


634 itraconazole
kidneys. Metabolized in liver. Primarily [Capsule]): Initially, 200 mg once daily.
excreted in urine. Not removed by hemo- May increase in increments of 100 mg/day
dialysis. Half-life: 16–26 hrs. up to 400 mg/day. Life-threatening in-
fections: 200 mg 3 times/day for first 3
LIFESPAN CONSIDERATIONS days of therapy. Continue for at least 3 mos.
Pregnancy/Lactation: Distributed in (Tolsura): 130 mg once daily; if no im-
breast milk. Children: Safety and efficacy provement or evidence of progressive fungal
not established. Elderly: Age-related renal infection, increase dose in 65 mg increments
impairment may require dosage adjustment. to a maximum of 260 mg/day given in 2 di-
vided doses. For life threatening infections,
INTERACTIONS give a loading dose of 130 mg 3 times/day
DRUG: May increase concentration/ for the first 3 days of treatment. Treatment
toxicity of aliskiren, calcium channel should be continued for 3 mos or greater.
–blocking agents (e.g., felodipine,
NIFEdipine), cycloSPORINE, digoxin, Aspergillosis
I dofetilide, eplerenone, ergot alkaloids, PO: ADULTS, ELDERLY: (Sporanox [Cap-
HMG-CoA reductase inhibitors (e.g., sule]): 200–400 mg daily for 3 mos.
lovastatin, simvastatin), midazolam, Life-threatening infections: 200 mg
sirolimus, tacrolimus, warfarin. 3 times/day for first 3 days of therapy.
Strong CYP3A4 inhibitors (e.g., clar- Continue 200–400 mg/day for at least
ithromycin, ketoconazole, ritonavir) 3 mos. (Tolsura): 130 mg 1–2 times/
may increase concentration/effect. Strong day. For life threatening infections, give a
CYP3A4 inducers (e.g., carbamaze- loading dose of 130 mg 3 times/day for
pine, phenytoin, rifampin) may decrease the first 3 days of treatment. Treatment
concentration/effect. May inhibit metabolism should be continued for at least 3 mos.
of DOCEtaxel, vinca alkaloids. Antacids,
H2 antagonists, proton pump inhibi- Esophageal Candidiasis
tors may decrease absorption. HERBAL: St. PO: ADULTS, ELDERLY: Swish 100–200 mg
John’s wort may decrease concentration/ (10–20 mL) in mouth for several seconds,
effect. FOOD: Grapefruit products may then swallow once daily for a minimum of 3
alter absorption. LAB VALUES: May increase wks. Continue for 2 wks after resolution of
serum alkaline phosphatase, bilirubin, ALT, symptoms. Maximum: 200 mg/day.
AST, LDH. May decrease serum potassium.
Oropharyngeal Candidiasis
AVAILABILITY (Rx) PO: ADULTS, ELDERLY: 200 mg (10 mL)
Capsules: (Sporanox): 100 mg. (Tolsura): oral solution, swish and swallow once
65 mg. Oral Solution: (Sporanox): 10 mg/ daily for 7–14 days.
mL. Onychomycosis (Fingernail)
ADMINISTRATION/HANDLING PO: ADULTS, ELDERLY: (Capsule): 200 mg
twice daily for 7 days, off for 21 days, re-
PO
peat 200 mg twice daily for 7 days.
• Give capsules with food (increases ab-
sorption). • Give solution on empty stom- Onychomycosis (Toenail)
ach. Swish vigorously in mouth, then swallow. PO: ADULTS, ELDERLY: (Tablet): 200 mg
INDICATIONS/ROUTES/DOSAGE once daily for 12 wks.
Note: Capsules/tablets are not bioequiv- Dosage in Renal/Hepatic Impairment
alent with oral solution. Use caution.
Blastomycosis, Histoplasmosis SIDE EFFECTS
PO: ADULTS, ELDERLY: (Sporanox Frequent (11%–9%): Nausea, rash.
underlined – top prescribed drug
ivabradine 635
Occasional (5%–3%): Vomiting, headache, tomatic chronic HF with left ventricular
diarrhea, hypertension, peripheral edema, ejection fraction less than or equal to
fatigue, fever. Rare (2% or less): Abdominal 35%, who are in sinus rhythm with a
pain, dizziness, anorexia, pruritus. resting heart rate greater than or equal
to 70 bpm, and either are on maximally
ADVERSE EFFECTS/TOXIC tolerated dose of beta blockers or have a
REACTIONS contraindication to beta blocker use.
Hepatitis (anorexia, abdominal pain, un-
usual fatigue/weakness, jaundiced skin/ PRECAUTIONS
sclera, dark urine) occurs rarely. Contraindications: Hypersensitivity to iv-
abradine. Acute decompensated HF, B/P
NURSING CONSIDERATIONS less than 90/50 mm Hg, sick sinus syn-
BASELINE ASSESSMENT drome; sinoatrial block or third-degree
AV block (unless a functional pacemaker
Determine baseline temperature, LFT. is present), resting heart rate less than
Assess allergies. Receive full medication 60 bpm prior to initiation, severe hepatic I
history (numerous contraindications/ impairment, pacemaker dependence
cautions). (heart rate maintained exclusively by a
INTERVENTION/EVALUATION pacemaker), concomitant use of strong
Assess for signs, symptoms of hepatic CYP3A4 inhibitors. Cautions: History of
dysfunction. Monitor LFT in pts with pre- atrial fibrillation, hypertension. Avoid con-
existing hepatic impairment. comitant use of dilTIAZem or verapamil.
Avoid use in pts with second-degree heart
PATIENT/ FAMILY TEACHING block (unless a functioning pacemaker is
• Take capsules with food, liquids if GI present). Pts at risk for bradycardia. Not
distress occurs. • Therapy will con- recommended with pacemakers set to rate
tinue for at least 3 mos, until lab tests, of 60 bpm or greater.
clinical presentation indicate infection is
controlled. • Immediately report un- ACTION
usual fatigue, yellow skin, dark urine, Reduces spontaneous pacemaker activ-
pale stool, anorexia, nausea, vomit- ity of the cardiac sinus node by blocking
ing. • Avoid grapefruit products. HCN channels that are responsible for
cardiac current, which regulates heart
rate. Does not affect ventricular repo-
larization or myocardial contractility.
ivabradine Also inhibits retinal current involved in
reducing bright light in retina. Thera-
eye-vab-ra-deen peutic Effect: Reduces heart rate.
(Corlanor)
PHARMACOKINETICS
uCLASSIFICATION Widely distributed. Metabolized in liver
PHARMACOTHERAPEUTIC: Hyper- and intestines. Protein binding: 70%.
polarization-activated cyclic nucle- Peak plasma concentration: 1 hr. Elimi-
otide-gated (HCN) channel blocker. nated in feces, urine (% not specified).
CLINICAL: Reduces risk of worsen- Half-life: 6 hrs.
ing HF.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: May cause
USES fetal harm. Females of reproductive po-
To reduce the risk of hospitalization for tential should use effective contracep-
worsening HF in pts with stable, symp- tion. Unknown if distributed in breast

Canadian trade name Non-Crushable Drug High Alert drug


636 ivabradine
milk. Must either discontinue drug or Heart Rate Dose Adjustment
discontinue breastfeeding. If treatment Greater than 60 Increase by 2.5 mg
is decided to be absolutely necessary, bpm (given twice daily)
pregnant pts should be closely moni- up to maximum
tored for destabilizing HF, esp. during dose of 7.5 mg
the first trimester. Pregnant women with daily.
chronic HF in the third trimester should 50–60 bpm Maintain dose.
be closely monitored for preterm birth. Less than 50 bpm Decrease by 2.5 mg
Children: Safety and efficacy not estab- or symptomatic (given twice daily);
bradycardia if current dose is
lished. Elderly: No age-related precau- 2.5 mg twice daily,
tions noted. permanently dis-
continue.
INTERACTIONS
DRUG: DilTIAZem, verapamil may in-
crease concentration/effect; may further Dosage in Renal Impairment
I increase risk of bradycardia. Strong Mild to moderate impairment: CrCl
CYP3A4 inhibitors (e.g., clarithro- 15 mL/min or greater: No dose adjust-
mycin, ketoconazole, ritonavir) ment. Severe impairment: CrCl less
may increase concentration/effect. than 15 mL/min: Use caution.
Strong CYP3A4 inducers (e.g., car- Dosage in Hepatic Impairment
BAMazepine, phenytoin, rifAMPin) Mild to moderate impairment: No
may decrease concentration/effect. dose adjustment. Severe impairment:
HERBAL: St. John’s wort may decrease
Contraindicated.
concentration/effect. FOOD: Grapefruit
products may increase concentration/ SIDE EFFECTS
effect. LAB VALUES: None significant. Occasional (10%–3%): Bradycardia, hy-
AVAILABILITY (Rx) pertension, phosphenes (visual distur-
bances, luminous phenomena), visual
Tablets: 5 mg, 7.5 mg. brightness.
ADMINISTRATION/HANDLING ADVERSE EFFECTS/TOXIC
PO REACTIONS
• Give with meals. May divide 5-mg tab- May increase risk of atrial fibrillation
let, providing 2.5-mg dose. (8.3% of pts). Bradycardia, sinus arrest,
INDICATIONS/ROUTES/DOSAGE or heart block may occur. Bradycar-
dia occurred in 10% of pts. Risk fac-
HF
tors for bradycardia may include sinus
PO: ADULTS, ELDERLY: Initially, 5 mg node dysfunction, conduction defects
twice daily for 14 days, then adjust dose (e.g., first- or second-degree AV block,
to resting heart rate of 50–60 bpm. Fur- bundle branch block), ventricular dys-
ther adjustments based on resting heart synchrony, or use of negative chrono-
rate and tolerability. Maximum: 7.5 mg tropic drugs. Phosphenes, a transient
twice daily. (See Dose Modification). enhanced brightness in the visual field
Pts with history of conduction defects, (which may include halos, stroboscopic
pts in whom bradycardia could lead to or kaleidoscopic effect, colored bright
hemodynamic compromise: Initiate lights, or multiple images) may occur.
therapy at 2.5 mg twice daily. Phosphenes are usually triggered by
Dose Modification sudden variations in light intensity and
Adjust dose to maintain a resting heart generally occur within the first 2 mos of
between 50–60 bpm as follows: treatment. Other adverse reactions such

underlined – top prescribed drug


ivacaftor 637
as angioedema, diplopia, erythema, hy-
potension, pruritus, rash, syncope, urti- ivacaftor
caria, vertigo, visual impairment occur
rarely. Overdose may lead to severe and eye-va-kaf-tor
prolonged bradycardia requiring tem- (Kalydeco)
porary cardiac pacing or infusion of IV
beta-stimulating agents. FIXED-COMBINATION(S)
Orkambi: ivacaftor/lumacaftor
NURSING CONSIDERATIONS (cystic fibrosis transmembrane con-
ductance regulator): 125 mg/200 mg.
BASELINE ASSESSMENT
Symdeko: ivacaftor/tezacaftor (cystic
Obtain baseline HR, B/P. Confirm nega- fibrosis transmembrane conduct-
tive pregnancy test before initiating ther- ance regulator): 50 mg/75 mg, 100
apy. Receive full medication history and mg/150 mg.
screen for interactions. Screen for con-
traindications as listed in Precautions. uCLASSIFICATION
I
Question history of atrial fibrillation, bra- PHARMACOTHERAPEUTIC: Cystic
dycardia, hypertension. fibrosis transmembrane conduct-
INTERVENTION/EVALUATION ance regulator potentiator. CLINI-
CAL: Cystic fibrosis agent.
Frequently monitor HR, B/P. Diligently
monitor for atrial fibrillation, bradycar-
dia, syncope. If symptomatic bradycardia USES
occurs, temporary cardiac pacing or in- A cystic fibrosis transmembrane regu-
fusion of beta-stimulating agents may be lator (CFTR) potentiator used for the
warranted. Immediately report suspected treatment of cystic fibrosis (CF) in pts 6
pregnancy. Monitor for hypersensitivity mos of age and older having one muta-
reaction. Monitor for visual changes. Ini- tion in the CFTR gene that is responsive
tiate fall precautions. to ­ivacaftor.
PATIENT/FAMILY TEACHING
PRECAUTIONS
• Take medication with meals. • Avoid
Contraindications: Hypersensitivity to
grapefruit products, herbal supplements
such as St. John’s wort. • Treatment ivacaftor. Cautions: Moderate to severe
may cause fetal harm. Female pts of re- hepatic/renal impairment.
productive potential should use effective ACTION
contraception during treatment. • Re-
port symptoms of low heart rate such as Potentiates a specific protein to facilitate,
confusion, dizziness, fatigue, fainting, regulate chloride ions, water transport.
low blood pressure, pallor. • Report In cystic fibrosis pts with a specific gene
symptoms of atrial fibrillation such as mutation (G551D), a defect in chloride
chest pressure, palpitations, shortness of and water transport results in formation
breath. • Treatment may cause lumi- of thick mucus in lungs. Therapeutic
nous phenomena (phosphenes), a tran- Effect: Improves lung function, fewer
sient visual brightness that may include respiratory exacerbations.
halos, light sensitivity, or colored bright PHARMACOKINETICS
lights. • Avoid tasks that require alert-
ness, motor skills until response to drug Readily absorbed. Peak concentration
is established. • Report allergic reac- occurs in 4 hrs. Metabolized in liver. Pro-
tions such as hives, itching, rash, tongue tein binding: 99%. Primarily excreted in
swelling. feces. Half-life: 12 hrs.

Canadian trade name Non-Crushable Drug High Alert drug


638 ivacaftor

LIFESPAN CONSIDERATIONS Concurrent Use with Moderate CYP3A4


Inhibitors (e.g., fluconazole)
Pregnancy/Lactation: Distributed in
PO: ADULTS, CHILDREN 6 YRS AND
breast milk. Children: Safety and effi-
OLDER: 150 mg once daily. CHILDREN 6
cacy not established in children younger
MOS TO YOUNGER THAN 6 YRS, WEIGHING
than 2 yrs. Elderly: No age-related pre-
14 KG OR MORE: 75-mg granule packet
cautions noted.
once daily. 7–13 KG: 50-mg granule packet
INTERACTIONS once daily. 5–6 KG: 25-mg granule packet
once daily.
DRUG: Strong CYP3A4 inducers
(e.g., carBAMazepine, rifAMPin) Concurrent Use with Strong CYP3A4
substantially decrease concentra- Inhibitors (e.g., clarithromycin,
tion/effects. Concurrent use not rec- ketoconazole)
ommended. Strong CYP3A4 in- PO: ADULTS, CHILDREN 6 YRS AND
hibitors (e.g., clarithromycin, OLDER: 150 mg twice wkly. CHILDREN 6
ketoconazole) significantly increase MOS TO YOUNGER THAN 6 YRS, WEIGHING
I concentration. Moderate CYP3A4 14 KG OR MORE: 75-mg granule packet
inhibitors (e.g., erythromycin, flu- twice wkly. 7–13 KG: 50-mg granule
conazole) may increase concentration packet twice wkly. 5–6 KG: 25-mg granule
and should not be given concurrently. packet twice wkly.
HERBAL: St. John’s wort may decrease
concentration/effect. Bitter orange Dosage in Renal Impairment
may increase concentration/effect. Mild to moderate impairment: No
FOOD: Grapefruit products, Seville dose adjustment. Severe impairment,
oranges should be avoided (increases ESRD: Use caution.
concentration). High-fat meals in-
crease absorption. LAB VALUES: May Dosage in Hepatic Impairment
increase serum ALT, AST. Mild impairment: No dose adjust-
ment. Moderate impairment: ADULTS,
AVAILABILITY (Rx) ELDERLY: 150 mg once daily. CHILDREN
Oral Granules: 25 mg, 50 mg, 75 mg. Tab- WEIGHING 14 KG OR MORE: 75 mg once
lets, Film-Coated: 150 mg. daily. CHILDREN WEIGHING LESS THAN 14
KG: 50 mg once daily. Severe impair-
ADMINISTRATION/HANDLING ment: 150 mg once daily or q48h. Use
PO caution.
• Give with a high-fat meal (e.g., eggs,
butter, peanut butter, cheese pizza). SIDE EFFECTS
Frequent (24%–10%): Headache, na-
INDICATIONS/ROUTES/ sal congestion, abdominal discomfort,
DOSAGE diarrhea, nausea, rash. Occasional
Cystic Fibrosis (6%–5%): Rhinitis, dizziness, arthral-
PO: ADULTS, CHILDREN 6 YRS AND gia, bacteria in sputum. Rare (4% or
OLDER: One 150-mg tablet q12h with fat- less): Myalgia, wheezing, acne.
containing food. Total daily dose: 300
mg. CHILDREN 6 MOS TO YOUNGER THAN ADVERSE EFFECTS/TOXIC
6 YRS, WEIGHING 14 KG OR MORE: (Gran-
REACTIONS
ules): 75-mg packet q12hr. CHILDREN Upper respiratory infection occurs in
6 MOS TO YOUNGER THAN 6 YRS, WEIGH- 22% of pts, nasopharyngitis in 15%. In-
ING 7–13 KG: 50-mg packet q12hr. CHIL- crease in ALT, AST occurs in 6% of pts.
DREN 6 MOS TO YOUNGER THAN 6 YRS,
WEIGHING 5–6 KG: 25-mg packet q12h.

underlined – top prescribed drug


ivosidenib 639

NURSING CONSIDERATIONS USES


Treatment of acute myeloid leukemia
BASELINE ASSESSMENT (AML) with a susceptible IDH1 mutation
If the pt’s genotype is unknown, an FDA- in adults with newly diagnosed AML who
cleared CF mutation test should be used are 75 yrs or older or who have comor-
to detect presence of a CFTR mutation. bidities that preclude use of intensive in-
Assess LFT prior to and periodically dur- duction chemotherapy. Treatment of AML
ing therapy. with a susceptible IDH1 mutation in
INTERVENTION/EVALUATION
adults with relapsed or refractory AML.
Patients who develop increased serum ALT, PRECAUTIONS
AST levels should be closely monitored un- Contraindications: Hypersensitivity to ivo-
til the abnormalities resolve. Dosing should sidenib. Cautions: Baseline leukopenia,
be interrupted if transaminases (serum hypotension; active infection, cardiac
ALT or AST) are greater than 5 times upper disease, hepatic/renal impairment, elec-
limit of normal. Transaminases should be trolyte imbalance; conditions predispos- I
obtained every 3 mos during the first year ing to infection (e.g., diabetes, renal
of treatment and annually thereafter. failure, immunocompromised pts, open
PATIENT/FAMILY TEACHING wounds); pts at risk for QTc interval
• Always take medication with fatty prolongation, cardiac arrhythmias (con-
food. • Avoid grapefruit products and Se- genital long QT syndrome, HF, QT inter-
ville oranges. • Adhere to routine labora- val–prolonging medications, hypokale-
tory testing as a part of treatment regi- mia, hypomagnesemia); concomitant use
men. • Report headache, diarrhea, rash, strong or moderate CYP3A inhibitors,
signs and symptoms of respiratory infection. strong CYP3A inducers; dehydration; pts
at high risk for tumor lysis syndrome
(high tumor burden).
ACTION
ivosidenib Inhibits IDH1 enzymes on mutant IDH1
eye-voe-sid-e-nib variants, decreasing 2-hydroxyglutarate
(Tibsovo) (2-HG) levels and restoring myeloid dif-
ferentiation. Therapeutic Effect: Re-
j BLACK BOX ALERT j Life- duces blast counts; increases percentage
threatening and/or fatal differen-
tiation syndrome with symptoms of myeloid cells. Inhibits tumor growth
including fever, dyspnea, hypoxia, and proliferation.
pulmonary infiltrates, pleural or
pericardial effusion, rapid weight PHARMACOKINETICS
gain or peripheral edema, hypoten-
sion, renal dysfunction may occur. Widely distributed. Metabolized in liver.
Initiate corticosteroid therapy and Protein binding: 92%–96%. Peak plasma
hemodynamic monitoring in pts concentration: 3 hrs. Steady state
suspected of differentiation syn- reached in 14 days. Excreted in feces
drome until symptoms resolve. (77%), urine (17%). Half-life: 93 hrs.
Do not confuse ivosidenib with
enasidenib, ibrutinib, idelalisib, LIFESPAN CONSIDERATIONS
imatinib or ixazomib. Pregnancy/Lactation: Avoid preg-
uCLASSIFICATION
nancy; may cause fetal harm. Recommen-
dations for contraception not specified.
PHARMACOTHERAPEUTIC: Isocitrate Unknown if distributed in breast milk.
dehydrogenase-1 (IDH1) inhibitor. Breastfeeding not recommended during
CLINICAL: Antineoplastic. treatment and for at least 30 days after
Canadian trade name Non-Crushable Drug High Alert drug
640 ivosidenib
discontinuation. Children: Safety and ef- Dose Modification
ficacy not established. Elderly: No age- Based on Common Terminology Criteria
related precautions noted. for Adverse Events (CTCAE).

INTERACTIONS Differentiation Syndrome


DRUG: Strong CYP3A4 inhibitors Withhold treatment if symptoms are se-
(e.g., clarithromycin, ketocon- vere and persist for more than 48 hrs
azole), moderate CYP3A4 inhibi- after initiation of corticosteroids. Re-
tors (e.g., erythromycin, dilTIAZem, sume treatment when symptoms improve
fluconazole) may increase concentra- to Grade 2 or less.
tion/effect. Strong CYP3A4 inducers Guillain-Barré Syndrome
(e.g., carBAMazepine, phenytoin, Permanently discontinue.
rifAMPin) may decrease concentration/
effect. QT interval–prolonging medi- Noninfectious Leukocytosis
cations (e.g., amiodarone, azithro- WBC count greater than 25,000
I mycin, citalopram, clarithromycin, cells/mm3 or absolute increase in
escitalopram, haloperidol) may in- total WBC count greater than 15,000
crease risk of QTc interval prolongation. cells/mm3 from baseline: If indicated,
May increase QT prolongation effect of treat with hydroxyurea and leukapher-
dronedarone. May decrease effect esis. Taper hydroxyurea after leukocyto-
of oral contraceptives. HERBAL: St. sis improves or resolves. If leukocytosis
John’s wort may decrease concentra- does not improve with hydroxyurea,
tion/effect. FOOD: High-fat meals may withhold treatment until resolved, then
increase concentration/effect. LAB VAL- resume at same dose.
UES: May increase serum alkaline phos-
phatase, ALT, AST, bilirubin, creatinine, QT Interval Prolongation
uric acid. May decrease Hgb, WBCs; se- QTc interval 481–500 msec: With-
rum magnesium, phosphate, potassium, hold treatment. Assess and replete elec-
sodium. trolyte levels. Assess and adjust con-
comitant use of medications known to
AVAILABILITY (Rx) cause QTc interval prolongation. When
Tablets: 250 mg. QTc interval prolongation improves to
480 msec or less, resume at same dose
ADMINISTRATION/HANDLING and monitor ECG at least wkly for 2
PO wks. QTc interval greater than 500
• Give without regard to low-fat msec: Withhold treatment. Assess and
food. • Do not give with a high-fat replete electrolyte levels. Assess and
meal. • Administer whole; do not adjust concomitant use of medications
break, cut, crush, or divide tablets. • known to cause QTc interval prolon-
Tablets cannot be chewed. • If vomiting gation. When QTc interval returns to
occurs after administration, give next within 30 msec of baseline or 480 msec
dose at regularly scheduled time. • If a or less, resume at reduced dose of 250
dose is missed, administer as soon as mg. QTc interval prolongation with
possible • Do not give a missed dose life-threatening arrhythmia: Perma-
within 12 hrs of next dose. nently discontinue.
INDICATIONS/ROUTES/DOSAGE Other Adverse Reactions
Acute Myeloid Leukemia Any Grade 3 or higher toxicity: With-
PO: ADULTS, ELDERLY: 500 mg once daily hold treatment until improved to Grade
for at least 6 mos. Continue until disease 2, then resume at reduced dose of 250
progression or unacceptable toxicity. mg. May increase to 500 mg if toxicities

underlined – top prescribed drug


ivosidenib 641
further improve to Grade 1 or 0. Recur- NURSING CONSIDERATIONS
rent Grade 3 or higher toxicity: Per-
manently discontinue. BASELINE ASSESSMENT

Concomitant Use of CYP3A4 Inhibitor


Obtain CBC, BMP, LFTs; ECG; pregnancy
If concomitant CYP3A4 inhibitor can- test in female pts of reproductive poten-
not be discontinued, reduce ivo- tial. Replete electrolytes if applicable.
sidenib dose to 250 mg. If CYP3A in- Confirm presence of IDH1 mutations in
hibitor is discontinued for 3–5 the blood or bone marrow. Assess ade-
half-lives, increase ivosidenib dose to quate hydration prior to initiation due to
500 mg. increased risk of tumor lysis syndrome,
diarrhea, vomiting. Screen for active in-
Dosage in Renal Impairment fection. Receive full medication history
Mild to moderate impairment: No (including herbal products) and screen
dose adjustment. Severe impairment: for interactions. Concomitant use of other
Not specified; use caution. medications may need to be adjusted.
Assess risk for QT interval prolongation, I
Dosage in Hepatic Impairment tumor lysis syndrome. Question history of
Mild to moderate impairment: No cardiac/hepatic/renal disease, cardiac ar-
dose adjustment. Severe impairment: rhythmias. Offer emotional support.
Not specified; use caution.
INTERVENTION/EVALUATION
SIDE EFFECTS Monitor CBC, BMP, LFTs at least wkly for
Frequent (39%–18%): Fatigue, asthenia, 4 wks, then every other wk for 4 wks,
arthralgia, diarrhea, dyspnea, edema, then monthly until discontinuation. Mon-
nausea, abdominal pain, mucositis, rash, itor CK levels wkly for at least 4 wks. An
pyrexia, cough, constipation, vomiting, increase of serum creatinine greater than
decreased appetite, myalgia. Occasional 0.4 mg/dL from baseline may indicate
(16%–12%): Chest pain, headache, neu- renal impairment. Monitor serum uric
ropathy, hypotension. acid level if tumor lysis syndrome (acute
renal failure, electrolyte imbalance, car-
ADVERSE EFFECTS/TOXIC diac arrhythmias, seizures) is suspected.
REACTIONS Monitor ECG at least wkly for 3 wks, then
Anemia, leukopenia is an expected re- monthly until discontinuation. If QT
sponse to therapy. Life-threatening interval–prolonging medications cannot
and/or fatal differentiation syndrome, be withheld, diligently monitor ECG; se-
a condition with rapid proliferation rum potassium, magnesium for QT inter-
and differentiation of myeloid cells, val prolongation, cardiac arrhythmias.
reported in 19%–25% of pts. QT inter- Monitor B/P for hypotension, esp. in pts
val prolongation with QTc interval taking antihypertensives. Monitor for
greater than 500 msec (9% of pts) and symptoms of differentiation syndrome
QTc interval greater than 60 msec (dyspnea, fever hypotension, hypoxia,
from baseline (14% of pts) have oc- pulmonary infiltrates, pleural or pericar-
curred. Guillain-Barré syndrome oc- dial effusion, rapid weight gain or pe-
curred in less than 1% of pts. Nonin- ripheral edema, renal dysfunction, or
fectious leukocytosis reported in 12% concomitant febrile neutropenic derma-
of pts. Tumor lysis syndrome may tosis). If differentiation syndrome is sus-
present as acute renal failure, hypocal- pected, initiate corticosteroids and he-
cemia, hyperuricemia, hyperphospha- modynamic monitoring until symptoms
temia. resolve for at least 3 days. Monitor for
symptoms of Guillain-Barré syndrome

Canadian trade name Non-Crushable Drug High Alert drug


642 ixabepilone
(dysphagia, dysarthria, dyspnea, motor
weakness, paresthesia, sensory altera- ixabepilone
tions). Diligently monitor for infection.
Assess skin for skin reactions, rash. ix-ab-ep-i-lone
Monitor daily pattern of bowel activity, (Ixempra)
stool consistency. Ensure adequate hy- j BLACK BOX ALERT jCombina-
dration, nutrition. tion therapy with capecitabine is
contraindicated in pts with serum
PATIENT/FAMILY TEACHING
ALT or AST greater than 2.5 times
upper limit of normal (ULN) or
• Treatment may depress your immune bilirubin greater than 1 times ULN
system response and reduce your ability due to increased risk of toxicity,
to fight infection. Report symptoms of in- neutropenia-related mortality.
fection such as body aches, chills, cough, uCLASSIFICATION
fatigue, fever. Avoid those with active in-
fection. • Report symptoms of bone PHARMACOTHERAPEUTIC: Epothilone
I marrow depression such as bruising, fa- microtubule inhibitor, antimitotic
tigue, fever, shortness of breath, weight agent. CLINICAL: Antineoplastic.
loss; bleeding easily, bloody urine or
stool. • Report palpitations, chest pain, USES
shortness of breath, dizziness, fainting;
may indicate arrhythmia. • Therapy Combination therapy with capecitabine
may cause life-threatening tumor lysis for treatment of metastatic or locally
syndrome (a condition caused by the advanced breast cancer in pts after fail-
rapid breakdown of cancer cells), which ure of anthracycline, taxane therapy. As
can cause kidney failure. Report de- monotherapy, treatment of metastatic or
creased urination, amber-colored urine; locally advanced breast cancer in pts af-
confusion, difficulty breathing, fatigue, ter failure of anthracycline, taxane, and
fever, muscle or joint pain, palpitations, capecitabine therapy. OFF-LABEL: Treat-
seizures, vomiting. • Treatment may ment of endometrial cancer.
cause life-threatening differentiation syn- PRECAUTIONS
drome as early as 2 days after starting
therapy. Report difficulty breathing, fever, Contraindications: Hypersensitivity to ixa-
low blood pressure, rapid weight gain, bepilone. Severe hypersensitivity r­eaction
swelling of the hands or feet, decreased (Grade 3 or 4) to Cremophor, baseline
urine output. • Report liver problems neutrophil count less than 1,500 cells/
(abdominal pain, bruising, clay-colored mm3 or platelet count less than 100,000
stool, amber- or dark-colored urine, yel- cells/mm3. Combination Capecitabine
lowing of the skin or eyes), kidney prob- Therapy: Serum ALT or AST greater
lems (decreased urine output, flank pain, than 2.5 times the upper limit of normal,
darkened urine), skin reactions (rash, bilirubin greater than 1 times the up-
skin eruptions). • There is a high risk per limit of normal. Cautions: Diabetes,
of interactions with other medications. existing moderate to severe neuropathy,
Do not take newly prescribed medica- history of cardiovascular disease. Mono-
tions unless approved by prescriber who therapy: Serum ALT or AST greater than
originally started treatment. • Avoid 5 times upper limit of normal bilirubin
grapefruit products, herbal supplements greater than 3 times upper limit of normal.
(esp. St. John’s wort). • Report sus- ACTION
pected pregnancy. Do not breast-
feed. • Drink plenty of fluids. • Avoid Binds directly on microtubules during
high-fat meals during administration. active stage of G2 and M phases of cell
cycle, preventing formation of microtu-

underlined – top prescribed drug


ixabepilone 643
bules, an essential part of the process of Rate of administration • Administer
separation of chromosomes. Therapeu- through an in-line filter of 0.2 to 1.2 mi-
tic Effect: Blocks cells in mitotic phase crons. • Infuse over 3 hrs. Administra-
of cell division, leading to cell death. tion must be completed within 6 hrs of
reconstitution.
PHARMACOKINETICS Storage • Refrigerate kit. • Prior to re-
Metabolized in liver. Protein binding: constitution, kit should be removed from
77%. Excreted in feces (65%), urine refrigerator and allowed to stand at room
(21%). Half-life: 52 hrs. temperature for approximately 30
min. • When vials are initially removed
LIFESPAN CONSIDERATIONS from refrigerator, a white precipitate may be
Pregnancy/Lactation: May cause fetal observed in the diluent vial. • This precipi-
harm. Unknown if distributed in breast tate will dissolve to form a clear solution
milk. Children: Safety and efficacy not once diluent warms to room tempera-
established. Elderly: Higher incidence ture. • Once diluted with lactated Ringer’s,
of severe adverse reactions in those older solution is stable at room temperature and I
than 65 yrs. room light for a maximum of 6 hrs.
INTERACTIONS INDICATIONS/ROUTES/DOSAGE
DRUG: Strong CYP3A4 Inhibitors b ALERT c An H1 antagonist (diphen-
(e.g., clarithromycin, ketoconazole, hydrAMINE 50 mg PO or equivalent) and
ritonavir) may increase concentra- an H2 antagonist (raNITIdine 150–300 mg
tion/effect. Strong CYP3A4 inducers PO or equivalent) must be given prior to
(e.g., carBAMazepine, phenytoin, beginning treatment with ixabepilone. Pts
rifAMPin) may decrease concentra- who experienced a previous hypersensitiv-
tion/effect. HERBAL: St. John’s wort ity reaction to ixabepilone require pretreat-
may decrease concentration/effect. ment with corticosteroids (e.g., dexametha-
FOOD: Grapefruit products may in- sone 20 mg IV 30 min before infusion, or
crease concentration/effect. LAB VAL- PO 1 hr before infusion) in addition to
UES: May increase serum ALT, AST, pretreatment with H1 and H2 antagonists.
bilirubin. May decrease WBCs, Hgb,
platelets. Breast Cancer (Monotherapy or in
Combination with Capecitabine)
AVAILABILITY (Rx) IV: ADULTS, ELDERLY: 40 mg/m2 infused
Injection, Solution: Kit:15-mg kit supplied over 3 hrs q3 wks. Maximum: 88 mg.
with diluent for Ixempra, 8 mL; 45 mg sup- Continue until disease progression or un-
plied with diluent for Ixempra, 23.5 mL. acceptable toxicity.

ADMINISTRATION/HANDLING Monotherapy Dosage Adjustments for


Hepatic Impairment
IV Mild Hepatic Impairment (ALT and AST
Reconstitution • Withdraw diluent Less Than 2.5 Times Upper Limit of Normal
and slowly inject into vial. • Gently [ULN] and Bilirubin Less Than 1 Time ULN)
swirl and invert until powder is com- IV: ADULTS, ELDERLY: 40 mg/m2 infused
pletely dissolved. • Further dilute with over 3 hrs q3 wks.
250 mL lactated Ringer’s. • Solution
may be stored in vial for a maximum of 1 Mild Hepatic Impairment (ALT and AST
hr at room temperature. • Final con- Greater Than 2.5 Times ULN and Less Than
centration for infusion must be between 10 Times ULN and Bilirubin Greater Than 1
0.2 mg/mL and 0.6 mg/mL. • Mix infu- Time ULN and Less Than 1.5 Times ULN)
sion bag by manual rotation. IV: ADULTS, ELDERLY: 32 mg/m2 infused
over 3 hrs q3 wks.
Canadian trade name Non-Crushable Drug High Alert drug
644 ixabepilone
Moderate Hepatic Impairment (ALT and edema, hand-foot syndrome (blister-
AST Less Than 10 Times ULN and Bilirubin ing/rash/peeling of skin on palms of
Greater Than 1.5 Times ULN and Less hands, soles of feet), pyrexia, dizzi-
Than 3 Times ULN) ness, pruritus, gastroesophageal reflux
IV infusion: ADULTS, ELDERLY: 20–30 disease (GERD), hot flashes, taste dis-
mg/m2 infused over 3 hrs q3 wks (initiate order, insomnia.
at 20 mg/m2; may increase up to a maxi-
mum of 30 mg/m2 in subsequent cycles ADVERSE EFFECTS/TOXIC
if tolerated). REACTIONS
Neuropathy occurs early during treat-
Dosage with Strong CYP3A4 Inhibitors/ ment; 75% of new onset or worsen-
Inducers ing neuropathy occurred during first
Inhibitors: Consider dose reduction to 3 cycles. Diabetics may be at increased
20 mg/m2. risk for severe neuropathy manifested
Inducers: Consider dose increase to 60 as Grade 4 neutropenia. Neutropenia,
I mg/m2. leukopenia occur commonly; anemia,
Dosage in Renal Impairment
thrombocytopenia occur rarely.
No dose adjustment. NURSING CONSIDERATIONS
Dose Modification BASELINE ASSESSMENT
Dosage adjustment based on grade of Question possibility of pregnancy. Ob-
neuropathy, hematologic conditions. tain baseline CBC, serum chemistries,
Hematologic
LFT before treatment begins as baseline
Neutrophils less than 500 cells/
and monitor for hepatotoxicity, periph-
mm3 for 7 days or longer: Reduce
eral neuropathy (most frequent cause of
dose by 20%. Neutropenic fever: Re- drug discontinuation). Offer emotional
duce dose by 20%. Platelets less than ­support.
25,000 cells/mm3 (less than 50,000 INTERVENTION/EVALUATION
cells/mm3 with bleeding): Reduce Monitor for symptoms of neuropathy
dose by 20%. (burning sensation, hyperesthesia, hypoes-
Neuropathy
thesia, paresthesia, discomfort, neuropathic
Grade 2 for 7 days or longer or Grade
pain). Assess hands and feet for erythema.
3 for less than 7 days: Reduce dose
Monitor CBC for evidence of neutropenia,
by 20%. Grade 3 for 7 days or lon- thrombocytopenia; LFT for hepatotoxicity.
ger: Discontinue treatment. Grade 3
Assess mouth for stomatitis, mucositis.
(other than neuropathy): Reduce dose PATIENT/FAMILY TEACHING
by 20%. Grade 4: Discontinue treatment. • Avoid crowds, those with known infec-
SIDE EFFECTS tion. • Avoid contact with those who
have recently received live virus vac-
Common (62%): Peripheral sensory neu- cine. • Do not have immunizations
ropathy. Frequent (56%–46%): Fatigue, without physician’s approval (drug low-
asthenia, myalgia, arthralgia, alopecia, ers resistance). • Promptly report fever
nausea. Occasional (29%–11%): Vomit- over 100.5°F, chills, numbness, tingling,
ing, stomatitis, mucositis, diarrhea, burning sensation, erythema of hands/
musculoskeletal pain, anorexia, con- feet.
stipation, abdominal pain, headache.
Rare (9%–5%): Skin rash, nail disorder,

underlined – top prescribed drug


ixazomib 645
reproductive potential should use ef-
ixazomib fective contraception during treatment
and up to 3 mos after discontinuation.
ix-az-oh-mib Unknown if distributed in breast milk.
(Ninlaro) Breastfeeding not recommended. Chil-
Do not confuse ixazomib with dren: Safety and efficacy not estab-
bortezomib, carfilzomib, idelal- lished. Elderly: No age-related precau-
isib, or ixekizumab. tions noted.
uCLASSIFICATION INTERACTIONS
PHARMACOTHERAPEUTIC: Protea- DRUG: Strong CYP3A inducers (e.g.,
some inhibitor. CLINICAL: Antineo- carBAMazepine, phenytoin, ri-
plastic. fAMPin) may decrease concentration/
effect; avoid use. May decrease effect
of oral contraceptives. HERBAL: St.
USES I
John’s wort may decrease concentra-
Treatment of multiple myeloma (in com- tion/effect. FOOD: High-fat meals may
bination with lenalidomide and dexa- decrease absorption/concentration. LAB
methasone) in pts who have received at VALUES: Expected to decrease neutro-
least 1 prior therapy. phils, platelets.
PRECAUTIONS AVAILABILITY (Rx)
Contraindications: Severe hypersensitiv- Capsules: 2.3 mg, 3 mg, 4 mg.
ity to ixazomib. Cautions: Baseline neu-
tropenia, thrombocytopenia; hepatic/ ADMINISTRATION/HANDLING
renal impairment, chronic peripheral PO
edema, predisposing factors to infec- • Capsule contents are hazardous; use
tion (e.g., diabetes, renal failure, open cytotoxic precautions during handling
wounds). Concomitant use of strong and disposal. • Administer capsule
CYP3A inducers not recommended. whole; do not break, cut, crush, or
open. • Give at least 1 hr before or 2
ACTION
hrs after food. • Give on the same day
Inhibits activity of beta 5 subunit of the each wk and at the same time that day. If
20S proteasome, leading to cell cycle ar- a dose is missed, do not administer
rest and tumor cell death (apoptosis). within 72 hrs of next scheduled
Therapeutic Effect: Inhibits tumor dose. • If vomiting occurs after dosing,
cells growth and metastasis. do not readminister; give dose at next
scheduled time.
PHARMACOKINETICS
Well absorbed following oral adminis- INDICATIONS/ROUTES/DOSAGE
tration. Widely distributed. Metabolized Multiple Myeloma
in liver. Protein binding: 99%. Peak Note: ANC should be 1,000 cells/mm3
plasma concentration: 1 hr. Excreted or greater, platelets 75,000 cells/mm3
in urine (62%), feces (22%). Not re- or greater, nonhematologic toxicities at
moved by hemodialysis. Half-life: 9.5 baseline or Grade 1 or less prior to initi-
days. ating a new cycle of therapy.
PO: ADULTS, ELDERLY: 4 mg once wkly
LIFESPAN CONSIDERATIONS
on days 1, 8, and 15 of 28-day cycle, in
Pregnancy/Lactation: Avoid preg- combination with lenalidomide 25 mg
nancy; may cause fetal harm/mal- daily (on days 1–21 of 28-day cycle) and
formations. Female and male pts of dexamethasone 40 mg (on days 1, 8, 15,

Canadian trade name Non-Crushable Drug High Alert drug


646 ixazomib
and 22 of 28-day cycle). Continue until resume lenalidomide at next lower dose
disease progression or unacceptable level (see manufacturer guidelines)
toxicity. and resume ixazomib at the same dose.
Recurrence of Grade 2 or 3 rash:
Dose Reduction Schedule Withhold ixazomib and lenalidomide
Initial dose: 4 mg. First dose reduc- until recovery to Grade 1 or 0, then re-
tion: 3 mg. Second dose reduction: sume ixazomib at reduced dose level and
2.3 mg. Unable to tolerate 2.3-mg resume lenalidomide at the same dose.
dose: Permanently discontinue. Grade 4 rash: Permanently discon-
tinue. Additional occurrences: Alter-
Dose Modification
nate dose modification of ixazomib and
Based on Common Terminology Criteria lenalidomide.
for Adverse Events (CTCAE).
Peripheral Neuropathy
Thrombocytopenia
Grade 1 (with pain) or Grade
Platelet count less than 30,000
I 2: Withhold ixazomib until resolved
cells/mm3: Withhold ixazomib and
lenalidomide until platelet count is to baseline or improved to Grade 1 or
30,000 cells/mm3 or greater, then re- 0 without pain (at prescriber’s discre-
sume ixazomib at the same dose and tion), then resume ixazomib at the same
resume lenalidomide at reduced dose dose. Grade 2 (with pain) or Grade
3: Withhold ixazomib until resolved to
level (see manufacturer guidelines).
Recurrence of platelet count less
baseline or improved to Grade 1 or 0
than 30,000 cells/mm3: Withhold
without pain (at prescriber’s discre-
ixazomib and lenalidomide until platelet tion), then resume ixazomib at reduced
count is 30,000 cells/mm3 or greater, dose level. Grade 4: Permanently dis-
then resume ixazomib at reduced continue.
dose level and resume lenalidomide Any Other Nonhematologic Toxicity
at the same dose. Additional occur- Grade 3 or 4: Withhold ixazomib un-
rences: Alternate dose modification of til resolved to baseline or improved to
ixazomib and lenalidomide. Grade 1 or 0 (at physician’s discretion),
Neutropenia then resume ixazomib at reduced dose
Absolute neutrophil count (ANC) level.
less than 500 cells/mm3: Withhold
Dosage in Renal Impairment
ixazomib and lenalidomide until ANC Mild to moderate impairment: Not
is 500 cells/mm3 or greater, then re- specified; use caution. Severe impair-
sume ixazomib at the same dose and ment (CrCl less than 30 mL/min),
resume lenalidomide at reduced dose end-stage renal disease: Reduce
level (see manufacturer guidelines). starting dose to 3 mg.
­Recurrence of ANC less than 500
cells/mm3: Withhold ixazomib and le- Dosage in Hepatic Impairment
nalidomide until ANC is 500 cells/mm3 or Mild impairment: No dose adjust-
greater, then resume ixazomib at reduced ment. Moderate to severe impair-
dose level and resume lenalidomide ment: Reduce starting dose to 3 mg.
at the same dose. Additional occur-
rences: Alternate dose modification of SIDE EFFECTS
ixazomib and lenalidomide. Frequent (42%–26%): Diarrhea, con-
stipation, nausea. Occasional (22%–
Rash
5%): Vomiting, back pain, blurry vision,
Grade 2 or 3 rash: Withhold lenalido- dry eye.
mide until resolved to Grade 1 or 0, then

underlined – top prescribed drug


ixazomib 647

ADVERSE EFFECTS/TOXIC occurs. Offer antiemetics for nausea,


REACTIONS antidiarrheals for diarrhea. Monitor
Neutropenia, thrombocytopenia are ex- for infection (esp. in pts with neutro-
pected responses to therapy. Thrombo- penia); dermal toxicity, skin rashes,
cytopenia reported in 78% of pts; neu- petechiae; peripheral neuropathy (with
tropenia in 67% of pts. Severe diarrhea or without pain); peripheral edema.
may lead to discontinuation of treat- Monitor daily pattern bowel activity,
ment. Peripheral neuropathy reported stool consistency. Monitor for side ef-
in 28% of pts (sensory neuropathies fects of dexamethasone (e.g., hyper-
were the most common type). Periph- glycemia, weight loss, decreased ap-
eral edema occurred in 28% of pts. petite), lenalidomide (see prescribing
Dermatologic toxicities including macu- information). Reversible posterior leu-
lopapular and macular rash may occur. koencephalopathy syndrome should be
Infectious processes including upper considered in pts with altered mental
respiratory tract infection (19% of pts), status, confusion, headache, seizures,
conjunctivitis (6% of pts) may occur. visual disturbances. Obtain visual acu- I
Other toxic reactions including neutro- ity if vision becomes blurry.
philic dermatosis, posterior reversible PATIENT/FAMILY TEACHING
encephalopathy, Stevens-Johnson syn-
• Treatment may depress your immune
drome, thrombotic thrombocytopenic
system and reduce your ability to fight
purpura, transverse myelitis, treatment-
infection. Report symptoms of infection
induced hepatotoxicity, tumor lysis syn-
such as body aches, chills, cough, fa-
drome, occur rarely.
tigue, fever. Avoid those with active infec-
NURSING CONSIDERATIONS tion. • Female and male pts of repro-
ductive potential should use effective
BASELINE ASSESSMENT contraception during treatment and up to
Obtain ANC, CBC (esp. platelet count), 3 mos after last dose. Do not breastfeed.
renal function test (in pts with renal Immediately report suspected preg-
impairment), LFT; pregnancy test in nancy. • Do not take ixazomib and
female pts of reproductive potential. dexamethasone at the same time. Take
Screen for active infection. Question dexamethasone with food to minimize GI
history of peripheral neuropathy, pe- upset. • Swallow capsules whole; do
ripheral edema, hepatic/renal impair- not chew, crush, or open. Take dose at
ment, current hemodialysis status. Re- least 1 hr before or 2 hrs after any
ceive full medication history including food. • Do not expose the capsule con-
herbal supplements. Offer emotional tents to the skin or eyes. If eyes are ex-
support. Assess hydration status. Obtain posed to the capsule powder, thoroughly
baseline visual acuity. Obtain dietary flush eyes with water. If skin is exposed to
consult for nutritional support. Offer the capsule powder, thoroughly wash
emotional support. skin with soap and water. • Treatment
may cause nerve pain; extreme sensitivity
INTERVENTION/EVALUATION to touch; muscle weakness; or prickling,
Monitor ANC, platelet count at least tingling, numbness in your hands and
monthly, more frequently during first 3 feet. • Report swelling of the legs, an-
cycles; LFT in pts with hepatic impair- kles, feet. • Report neurologic changes
ment. Consider concomitant granulo- such as blurry vision, confusion, head-
cyte colony-stimulating factor (e.g., ache, seizures; may indicate life-threat-
filgrastim, pegfilgrastim) in pts with ening brain swelling. • Treatment may
neutropenia. Monitor for dehydra- increase risk of bleeding. • Do not take
tion, electrolyte imbalance if diarrhea herbal supplements, esp. St. John’s wort.

Canadian trade name Non-Crushable Drug High Alert drug


648 ixekizumab
days. Steady state reached in 8–10 wks.
ixekizumab Elimination not specified. Half-life: 13
days.
ix-ee-kiz-ue-mab
(Taltz) LIFESPAN CONSIDERATIONS
Do not confuse ixekizumab Pregnancy/Lactation: Unknown if dis-
with daclizumab, eculizumab, tributed in breast milk. However, human
gevokizumab, secukinumab, or immunoglobulin G is present in breast
ustekinumab. milk and is known to cross placenta.
Children: Safety and efficacy not estab-
uCLASSIFICATION
lished. Elderly: No age-related precau-
PHARMACOTHERAPEUTIC: Human tions noted.
interleukin-17A antagonist. Mono-
clonal antibody. CLINICAL: Antipso- INTERACTIONS
riasis agent. DRUG: May decrease therapeutic re-
I sponse of BCG (intravesical), live
vaccines. May enhance the adverse/toxic
USES
effects of belimumab, natalizumab,
Treatment of moderate to severe plaque live vaccines. HERBAL: Echinacea
psoriasis in adults who are candidates may decrease effect. FOOD: None known.
for systemic therapy or phototherapy. LAB VALUES: May decrease neutrophils,
Treatment of active psoriatic arthritis in platelets. May decrease diagnostic effect
adults. Treatment of active ankylosing of Coccidioides immitis skin test.
spondylitis.
AVAILABILITY (Rx)
PRECAUTIONS
Auto-injector Pen: 80 mg/mL. Prefilled
Contraindications: Hypersensitivity to Syringe: 80 mg/mL.
ixekizumab. Cautions: Baseline neutro-
penia, thrombocytopenia; inflammatory ADMINISTRATION/HANDLING
bowel disease (Crohn’s disease, ulcerative SQ
colitis), HIV infection, concomitant immu- • Follow instructions for preparation
nosuppressant therapy, conditions predis- according to manufacturer guide-
posing to infection (e.g., diabetes, renal lines. • Remove auto-injector or pre-
failure, open wounds), pts who have been filled syringe from refrigerator and allow
exposed to tuberculosis. Concomitant use to warm to room temperature (approx.
of live vaccines not recommended. 30 mins) with needle cap intact. • Vi-
ACTION sually inspect for particulate matter or
discoloration. Solution should appear
Binds to and inhibits interaction of
clear, colorless to slightly yellow in color.
interleukin-17A receptor, a cytokine
Do not use if solution is cloudy, discol-
that is involved in inflammatory and im-
ored, or if visible particles are observed.
mune response. May reduce epidermal
Administration • Insert needle sub-
neutrophils in psoriatic plaques. Thera-
cutaneously into upper arms, outer thigh,
peutic Effect: Alters biologic immune
or abdomen, and inject solution. • Do
response; inhibits release of proinflam-
not inject into areas of active skin disease
matory cytokines and chemokines.
or injury such as sunburns, skin rashes,
PHARMACOKINETICS inflammation, skin infections, or active
psoriasis. • Rotate injection sites.
Widely distributed. Degraded into small
Storage • Refrigerate until time of
peptides and amino acids via catabolic
use. • Do not freeze. • Do not shake.
pathway. Peak plasma concentration: 4
• Protect from light.

underlined – top prescribed drug


ixekizumab 649

INDICATIONS/ROUTES/DOSAGE latent infection prior to initiating treat-


Ankylosing Spondylitis ment and periodically during therapy.
SQ: ADULTS, ELDERLY: 160 mg (two 80-mg Induration of 5 mm or greater with tu-
injections) once, then 80 mg q4wks. berculin skin testing should be consid-
ered a positive test result when assess-
Plaque Psoriasis ing if treatment for latent tuberculosis
SQ: ADULTS, ELDERLY: Initially, 160 mg is necessary. Consider administration of
(two injections of 80 mg) once, then 80 age-appropriate immunizations (if appli-
mg at wks 2, 4, 6, 8, 10, 12, then 80 mg cable) before initiation. Question history
once q4wks. of Crohn’s disease, ulcerative colitis, hy-
persensitivity reaction. Conduct derma-
Psoriatic Arthritis tologic exam; record characteristics of
Note: For pts with coexisting plaque pso- psoriatic lesions.
riasis, use dosage for plaque psoriasis.
SQ: ADULTS, ELDERLY: 160 mg once, INTERVENTION/EVALUATION
then 80 mg q4wks. May give alone or in Monitor for symptoms of tuberculosis, in- I
combination with conventional disease- cluding pts who tested negative for latent
modifying antirheumatic drugs (e.g., tuberculosis infection prior to initiating
methotrexate). therapy. Interrupt or discontinue treat-
ment if serious infection, opportunistic
Dosage in Renal/Hepatic Impairment infection, or sepsis occurs, and initiate
Not specified; use caution. appropriate antimicrobial therapy. Assess
SIDE EFFECTS skin for improvement of lesions. Monitor
for hypersensitivity reaction, symptoms of
Occasional (17%): Injection site reactions inflammatory bowel disease.
(pain, erythema). Rare (2%): Nausea.
PATIENT/FAMILY TEACHING
ADVERSE EFFECTS/TOXIC • A healthcare provider will show you
REACTIONS how to properly prepare and inject your
May increase risk of infection including medication. You must demonstrate cor-
tuberculosis. Infections including upper rect preparation and injection techniques
respiratory tract infection (14% of pts), na- before using medication at home.
sopharyngitis (14% of pts), tinea infections • Treatment may depress your immune
(2% of pts) have occurred. Cytopenias in- system response and reduce your ability
cluding neutropenia (11% of pts), throm- to fight infection. Report symptoms of
bocytopenia (3% of pts) were reported. infection such as body aches, chills,
May cause exacerbation of Crohn’s disease cough, fatigue, fever. Avoid people with
and ulcerative colitis. Hypersensitivity reac- active infection. • Do not receive live
tions, including angioedema, occur rarely. vaccines. • Expect frequent tuberculo-
Immunogenicity (auto-ixekizumab anti- sis screening. • Report travel plans to
bodies) occurred in less than 9% of pts. possible endemic areas. • Immediately
report difficulty breathing, itching, hives,
NURSING CONSIDERATIONS rash, swelling of the face or tongue; may
BASELINE ASSESSMENT indicate allergic reaction. • Treatment
Obtain CBC in pts with known history of may cause worsening of Crohn’s disease
neutropenia, thrombocytopenia. Screen or cause inflammatory bowel disease.
for active infection. Pts should be evalu- Report abdominal pain, diarrhea, weight
ated for active tuberculosis and tested for loss.

Canadian trade name Non-Crushable Drug High Alert drug


650 ketorolac
fluid retention, HF, renal impairment, in-
ketorolac flammatory bowel disease, smoking, use of
alcohol, elderly, debilitated.
kee-toe-role-ak
(Acular, Acular LS, Acuvail, Apo- ACTION
Ketorolac , Sprix, Toradol ) Inhibits COX-1 and COX-2 enzymes, re­
j BLACK BOX ALERT j Increased sulting in decreased prostaglandin syn­thesis;
risk of serious cardiovascular reduces prostaglandin levels in aqueous hu-
thrombotic events, including mor. Therapeutic Effect: Produces anal-
myocardial infarction, CVA. In-
creased risk of severe GI reactions, gesic, antipyretic, anti-inflammatory effect;
including ulceration, bleeding, reduces intraocular inflammation.
perforation.
Do not confuse Acular with PHARMACOKINETICS
Acthar or Ocular, ketorolac Well absorbed (100%) following oral
with Ketalar, or Toradol with administration. Protein binding: 99%.
Foradil, Inderal, TEGretol, or Metabolized in liver. Primarily excreted
traMADol. in urine. Not removed by hemodialysis.
K Half-life: 5–9 hrs (increased in renal
uCLASSIFICATION impairment, in elderly).
PHARMACOTHERAPEUTIC: NSAID.
CLINICAL: Analgesic, intraocular anti-­ LIFESPAN CONSIDERATIONS
inflammatory. Pregnancy/Lactation: Unknown if
dis­tributed in breast milk. Avoid use dur-
ing third trimester (may adversely affect
USES fetal cardiovascular system: premature
PO: injection, nasal: Short-term (5 closure of ductus arteriosus). Children:
days or less) relief of mild to moderate Safety and efficacy not established, but doses
pain. Ophthalmic: Relief of ocular itch- of 0.5 mg/kg have been used. ­Elderly: GI
ing due to seasonal allergic conjunctivi- bleeding, ulceration more likely to cause se-
tis. Treatment postop for inflammation rious adverse effects. Age-related renal im-
following cataract extraction, pain fol- pairment may increase risk of hepatic/renal
lowing incisional refractive surgery. OFF- toxicity; decreased dosage recommended.
LABEL: Prevention, treatment of ocular
inflammation (ophthalmic form). INTERACTIONS
DRUG: May decrease effects of antihy­
PRECAUTIONS pertensives (e.g., amLODIPine, lisin­
Contraindications: Hypersensitivity to ke­ opril), diuretics (e.g., furosemide,
torolac, aspirin, or other NSAIDs. Intra- HCTZ). Aspirin, NSAIDs, other salicy-
cranial bleeding, hemorrhagic diathesis, lates may increase risk of GI side effects,
incomplete hemostasis, high risk of bleed- bleeding. May increase risk of bleeding
ing; concomitant use of aspirin, NSAIDs, with heparin, oral anticoagulants
probenecid, or pentoxifylline; labor and (e.g., warfarin). May increase concen-
delivery, advanced renal impairment or tration, risk of toxicity of lithium. May
risk of renal failure, active or history of increase effect of apixaban, dabigatran,
peptic ulcer disease, chronic inflammation edoxaban, rivaroxaban. Bile acid se-
of GI tract, recent or history of GI bleeding/ questrants (e.g., cholestyramine) may
ulceration. Perioperative pain in setting of decrease absorption/effect. May increase
CABG surgery. Prophylaxis before major nephrotoxic effect of cycloSPORINE.
surgery. Cautions: Hepatic impairment, HERBAL: Glucosamine, herbs with
history of GI tract disease, asthma, coagu- anti­coagulant/antiplatelet properties
lation disorders, receiving anticoagulants, (e.g., garlic, ginger, ginseng, ginkgo

underlined – top prescribed drug


ketorolac 651
biloba) may increase concentration/ef- Pain Management
fect. FOOD: None known. LAB VALUES: PO: ADULTS, ELDERLY: Initially, 20 mg
May prolong bleeding time. May increase (10 mg for elderly), then 10 mg q4–6h.
serum ALT, AST, BUN, potassium, creati- Maximum: 40 mg/24 hrs.
nine. IM: ADULTS YOUNGER THAN 65 YRS: 60
mg once or 30 mg q6h. Maximum: 120
AVAILABILITY (Rx) mg/24 hrs. ADULTS 65 YRS AND OLDER, PTS
Injection Solution: 15 mg/mL, 30 mg/ WITH RENAL IMPAIRMENT, PTS WEIGHING
mL. Nasal Spray: (Sprix): 1.7-g bottle LESS THAN 50 KG: 30 mg once or 15 mg
provides 8 sprays (15.75 mg/spray). q6h. Maximum: 60 mg/24 hrs.
Ophthalmic Solution: (Acular LS): 0.4%, IV: ADULTS YOUNGER THAN 65 YRS: 30
(Acuvail): 0.45%, (Acular): 0.5%. mg once or 30 mg q6h. Maximum: 120
T­ ablets: 10 mg. mg/24 hrs. ADULTS 65 YRS AND OLDER, PTS
WITH RENAL IMPAIRMENT, PTS WEIGHING
ADMINISTRATION/HANDLING LESS THAN 50 KG: 15 mg once or 15 mg

IV
q6h. Maximum: 60 mg/24 hrs.
Nasal spray: ADULTS YOUNGER THAN
• Give undiluted as IV push. • Give 65 YRS, PTS WEIGHING 50 KG OR MORE: K
over at least 15 sec. One spray (15.75 mg) in each nostril (to-
tal dose: 31.5 mg) q6-8h. Maximum dose:
IM Four sprays (126 mg/day). ADULTS 65 YRS
• Give deep IM slowly into large muscle AND OLDER, PTS WEIGHING LESS THAN 50
mass. KG: One spray (15.75 mg) in each nostril
(total dose: 15.75 mg) q6-8h. Maximum
PO
dose: Four sprays (63 mg/day).
• Give with food, milk, antacids if GI
distress occurs. Allergic Conjunctivitis
Ophthalmic: ADULTS, ELDERLY, CHIL-
Ophthalmic
DREN 2 YRS AND OLDER: 1 drop (0.5%)
• Place gloved finger on lower eyelid 4 times/day.
and pull out until pocket is formed be-
tween eye and lower lid. Place prescribed Cataract Extraction
number of drops into pocket. • In- Ophthalmic: ADULTS, ELDERLY: 1 drop
struct pt to close eye gently for 1–2 min (0.5%) 4 times/day. Begin 24 hrs after
(so that medication will not be squeezed surgery and continue for 2 wks.
out of the sac) and to apply digital pres-
sure to lacrimal sac at inner canthus for Corneal Refractive Surgery
1 min to minimize system absorption. Ophthalmic: ADULTS, ELDERLY: 1 drop
(0.4%) 4 times/day for up to 4 days after
IV INCOMPATIBILITIES surgery.
Promethazine (Phenergan).
Dosage in Renal Impairment
IV COMPATIBILITIES See dosage section.
FentaNYL (Sublimaze), HYDROmorphone
Dosage in Hepatic Impairment
(Dilaudid), morphine, nalbuphine (Nu­
bain). Use caution.

INDICATIONS/ROUTES/DOSAGE SIDE EFFECTS


Note: Total duration is 5 days (paren- Frequent (17%–12%): Headache, nausea,
teral and oral). Do not increase dose/ abdominal cramps/pain, dyspepsia. Occa-
sional (9%–3%): Diarrhea. Nasal: Nasal
frequency; supplement with low-dose
opioids if needed. discomfort, rhinalgia, increased

Canadian trade name Non-Crushable Drug High Alert drug


652 ketorolac
lacrimation, throat irritation, rhinitis. INTERVENTION/EVALUATION
Ophthalmic: Transient stinging, burn- Monitor renal function, LFT, urinary
ing. Rare (3%–1%): Constipation, vomit- output. Monitor daily pattern of bowel
ing, ­flatulence, stomatitis. Ophthalmic: activity, stool consistency. Observe for
Ocular irritation, allergic reactions occult blood loss. Assess for therapeutic
(manifested by pruritus, stinging), su- response: relief of pain, stiffness, swell-
perficial ocular infection, keratitis. ing; increased joint mobility; reduced
joint tenderness; improved grip strength.
ADVERSE EFFECTS/TOXIC Monitor for bleeding (may also occur
REACTIONS with ophthalmic route due to systemic
Peptic ulcer, GI bleeding, gastritis, severe he- absorption).
patic reaction (cholestasis, jaundice) occur
rarely. Nephrotoxicity (glomerular nephritis, PATIENT/ FAMILY TEACHING
interstitial nephritis, nephrotic syndrome) • Avoid aspirin, alcohol. • Report ab-
may occur in pts with preexisting renal im- dominal pain, bloody stools, or vomiting
pairment. Acute hypersensitivity reaction (fe- blood. • If GI upset occurs, take with
ver, chills, joint pain) occurs rarely. food, milk. • Ophthalmic: Transient
K stinging, burning may occur upon instil-
NURSING CONSIDERATIONS lation. • Do not administer while wear-
BASELINE ASSESSMENT
ing soft contact lenses.
Assess onset, type, location, duration of
pain. Obtain baseline renal/hepatic func-
tion tests.

underlined – top prescribed drug


labetalol 653
PHARMACOKINETICS
labetalol Route Onset Peak Duration
la-bayt-a-lol PO 0.5–2 hrs 2–4 hrs 8–12 hrs
IV 2–5 min 5–15 min 2–4 hrs
(Trandate )
Do not confuse labetalol with Incompletely absorbed from GI tract.
atenolol, betaxolol, metoprolol Bioavailability: 25%. Protein binding:
or propranolol, or Trandate 50%. Metabolized in liver. Primarily ex­
with traMADol or TRENtal. creted in urine. Not removed by hemodi-
alysis. Half-life: 6–8 hrs.
FIXED-COMBINATION(S)
Normozide: labetalol/hydroCHLO- LIFESPAN CONSIDERATIONS
ROthiazide (a diuretic): 100 mg/25 Pregnancy/Lactation: Drug crosses
mg, 200 mg/25 mg, 300 mg/25 mg. placenta. Small amount distributed in
breast milk. Children: Safety and ef-
uCLASSIFICATION
ficacy not established. Elderly: Age-
PHARMACOTHERAPEUTIC: Alpha-, related peripheral vascular disease
beta-adrenergic blocker. CLINICAL: may increase susceptibility to de-
Antihypertensive. creased peripheral circulation. May
have increased risk of orthostatic L
hypotension.
USES
Management of hypertension. IV for severe INTERACTIONS
hypertension. OFF-LABEL: Management of DRUG: May decrease effects of beta2-
preeclampsia, severe hypertension in preg- adrenergic agonists (e.g., arfor-
nancy, hypertension during acute ischemic moterol, salmeterol), theophylline.
stroke, pediatric hypertension. Dronedarone, rivastigmine may
increase bradycardic effect. May in-
PRECAUTIONS crease bradycardic effect of fingolimod.
Contraindications: Hypersensitivity to la- HERBAL: Herbals with hypertensive
betalol. Bronchial asthma, history of ob- properties (e.g., licorice, yohimbe)
structive airway disease, cardiogenic or hypotensive properties (e.g., gar-
shock, uncompensated HF, second- or lic, ginger, ginkgo biloba) may alter
third-degree heart block (except in pts effects. FOOD: None known. LAB VAL-
with functioning pacemaker), severe UES: May increase serum antinuclear
bradycardia, conditions associated with antibody titer (ANA), BUN, LDH, alkaline
severe, prolonged hypotension. Cau- phosphatase, bilirubin, creatinine, po-
tions: Compensated HF, severe anaphy- tassium, triglycerides, lipoprotein, uric
laxis to allergens, myasthenia gravis, acid, ALT, AST.
psychiatric disease, hepatic impairment,
pheochromocytoma, diabetes; concur- AVAILABILITY (Rx)
rent use with digoxin, verapamil, or dil- 5 mg/mL. Tablets:
Injection Solution:
TIAZem; arterial obstruction, elderly. Pts 100 mg, 200 mg, 300 mg.
with peripheral vascular disease, Rayn-
aud’s disease. ADMINISTRATION/HANDLING
ACTION IV
Blocks alpha-1, beta-1, beta-2 (large b ALERT c Prolonged duration of action:
doses) adrenergic receptor sites. Thera- Monitor several hrs after administration.
peutic Effect: Decreases peripheral vascu- Excessive administration may result in pro-
lar resistance, B/P. longed hypotension and/or bradycardia.

Canadian trade name Non-Crushable Drug High Alert drug


654 labetalol
Reconstitution • For IV infusion, di- mg may be given at 10-min intervals, up
lute in D5W to provide concentration of to total dose of 300 mg. CHILDREN: 0.2–1
1–2 mg/mL. mg/kg/dose. Maximum: 40 mg/dose.
Rate of administration • For IV push, IV infusion: ADULTS: Initially, 0.5–2 mg/
administer at a rate of 10 mg/min. • For min up to 10 mg/min. CHILDREN: 0.25–3
IV infusion, administer at rate of 2 mg/min mg/kg/hr. Maximum: 3 mg/kg/hr.
initially. Rate is adjusted according to
B/P. • Monitor B/P immediately before Dosage in Renal Impairment
and q5–10min during IV administration No dose adjustment.
(maximum effect occurs within 5 min).
Dosage in Hepatic Impairment
Storage • Store at room tempera-
ture. • After dilution, IV solution is sta- Use caution.
ble for 72 hrs. • Solution appears SIDE EFFECTS
clear, colorless to light yellow. • Dis-
card if discolored or precipitate forms. Frequent (20%–11%): Drowsiness, dizzi-
ness, excessive fatigue. Occasional (10%
PO or less): Dyspnea, peripheral edema, de-
• Give without regard to food. • Tab- pression, anxiety, constipation, diarrhea,
lets may be crushed. nasal congestion, weakness, diminished
L sexual function, transient scalp tingling,
IV INCOMPATIBILITIES insomnia, nausea, vomiting, abdominal
Amphotericin B complex (Abelcet, AmBi- discomfort. Rare: Altered taste, dry eyes,
some, Amphotec), ceftaroline (Teflaro), increased urination, paresthesia.
cefTRIAXone (Rocephin), furosemide
(Lasix), heparin, nafcillin (Nafcil). ADVERSE EFFECTS/TOXIC
REACTIONS
IV COMPATIBILITIES May precipitate, aggravate HF due to de-
Amiodarone (Cordarone), calcium glu- creased myocardial stimulation. Abrupt
conate, dexmedetomidine (Precedex), withdrawal may precipitate myocardial
dilTIAZem (Cardizem), DOBUTamine ischemia, producing chest pain, diapho-
(Dobutrex), DOPamine (Intropin), enala- resis, palpitations, headache, tremor.
pril (Vasotec), fentaNYL (Sublimaze), May mask signs, symptoms of acute hy-
HYDROmorphone (Dilaudid), lidocaine, poglycemia (tachycardia, B/P changes)
LORazepam (Ativan), magnesium sulfate, in diabetic pts. Rapid reduction of blood
midazolam (Versed), milrinone (Prima- pressure may cause CVA, optic nerve in-
cor), morphine, nitroglycerin, norepi- farction, ischemic changes on ECG. May
nephrine (Levophed), potassium chloride, cause severe orthostatic hypotension.
potassium phosphate, propofol (Diprivan).
NURSING CONSIDERATIONS
INDICATIONS/ROUTES/DOSAGE
Hypertension BASELINE ASSESSMENT
PO: ADULTS, ELDERLY: Initially, 100 mg Assess baseline renal function, LFT. Assess
twice daily. Adjust in increments of 100 mg B/P, apical pulse immediately before drug
twice daily q2–3days. Usual dose: 200–800 administration (if pulse is 60/min or less or
mg/day in 2 divided doses. May require up systolic B/P is lower than 90 mm Hg, with-
to 2,400 mg/day. CHILDREN: 1–3 mg/kg/ hold medication, contact physician). Ques-
day in 2 divided doses. Maximum: 10– tion history of bradycardia, HF, second- or
12 mg/kg/day up to 1,200 mg/day. third-degree heart block, myasthenia gravis.

Severe Hypertension, Hypertensive Crisis INTERVENTION/EVALUATION


IV: ADULTS: Initially, 10–20 mg (bolus Monitor B/P for hypotension. Assess pulse
over 2 min). Additional doses of 40–80 for quality, irregular rate, bradycardia.

underlined – top prescribed drug


lacosamide 655
Monitor ECG for cardiac arrhythmias. As- ACTION
sist with ambulation if dizziness occurs. Selectively enhances slow inactiva-
Assess for evidence of HF: dyspnea (par- tion of sodium channels, stabilizing
ticularly on exertion or lying down), night hyperexcitable neuronal membranes
cough, peripheral edema, distended neck and inhibits neuronal firing. Thera-
veins. Monitor I&O (increase in weight, peutic Effect: Reduces seizure
decrease in urine output may indicate HF). frequency.
PATIENT/FAMILY TEACHING PHARMACOKINETICS
• Do not discontinue drug except upon Completely absorbed following PO ad-
advice of physician (abrupt discontinua- ministration. Protein binding: 15%. Peak
tion may precipitate heart failure). plasma concentration: 1–4 hrs after oral
• Slowly go from lying to standing. dosing and is reached at the end of IV infu-
• Compliance with therapy regimen is sion. Primarily excreted in urine. Steady-
essential to control hypertension, arrhyth- state levels achieved in 3 days. Removed by
mias. • Avoid tasks that require alert- hemodialysis. Half-life: 13 hrs.
ness, motor skills until response to drug is
established. • Report shortness of LIFESPAN CONSIDERATIONS
breath, excessive fatigue, weight gain, pro- Pregnancy/Lactation: Use in preg-
longed dizziness, headache. • Do not nancy if benefits outweigh risk. Un- L
use nasal decongestants, OTC cold prepa- known if distributed in breast milk.
rations (stimulants) without physician ap- Children: Safety and efficacy not es-
proval. • Limit alcohol. tablished in pts younger than 17 yrs.
Elderly: No age-related precautions
noted.
lacosamide INTERACTIONS
DRUG: None significant. HERBAL: None
la-koe-sa-myde significant. FOOD: None known. LAB
(Vimpat) VALUES: May increase serum ALT;
Do not confuse lacosamide with proteinuria.
zonisamide.
AVAILABILITY (Rx)
uCLASSIFICATION Injection Solution: 10 mg/mL (20 mL).
PHARMACOTHERAPEUTIC: Succi­ Oral Solution: 10 mg/mL.
nimide (Schedule V). CLINICAL: Tablets: 50 mg, 100 mg, 150 mg,
Anticonvulsant. 200 mg.
ADMINISTRATION/HANDLING
USES PO
Monotherapy or adjunctive therapy for • Give without regard to food. • Do
treatment of partial-onset seizures in not break, crush, dissolve, or divide film-
pts 4 yrs and older. coated tablets. • Oral solution should
be administered with a calibrated mea-
PRECAUTIONS suring device. • Discard any unused
Contraindications: Hypersensitivity to laco­ portion after 7 wks.
samide. Cautions: Renal/hepatic impair- IV
ment, cardiac conduction problems (e.g.,
marked first-degree AV block, second- • Appears as a clear, colorless solu-
degree or higher AV block, sick sinus syn- tion. • Discard unused portion or if pre-
drome without pacemaker), myocardial cipitate or discoloration is present. May give
ischemia, HF, pts at risk of suicide. without further dilution. • If mixing with
Canadian trade name Non-Crushable Drug High Alert drug
656 lacosamide
diluent, may be stored for 24 hrs at room Dosage in Renal Impairment
temperature. Infuse over 30–60 min. Use caution when titrating. Mild to mod-
erate impairment: No dose adjustment.
IV COMPATIBILITIES Severe impairment, end-stage renal
0.9% NaCl, D5W, lactated Ringer’s. disease: Maximum: 300 mg/day.

INDICATIONS/ROUTES/DOSAGE Dosage in Hepatic Impairment


Note: IV dose is same as oral dose. May Use caution when titrating. Mild to
give undiluted or mixed in compatible di- moderate impairment: Maximum:
luent and infused over 30–60 min. 300 mg/day. Severe impairment: Not
recommended.
Partial-Onset Seizures
Monotherapy SIDE EFFECTS
PO/IV: ADULTS, ELDERLY: Initially, 100 mg Frequent (31%–13%): Dizziness, head-
twice daily. May increase by 50 mg twice daily ache. Occasional (11%–5%): Nausea,
at wkly intervals. Maintenance: 150–200 double vision, vomiting, fatigue, blurred
mg twice daily. CHILDREN 4–17 YRS, WEIGH- vision, ataxia, tremor, nystagmus. Rare
ING 50 KG OR MORE: Initially, 50 mg twice (4%–2%): Vertigo, diarrhea, gait distur-
daily. May increase by 50 mg twice daily at bances, memory impairment, depres-
L wkly intervals. Maintenance: 150–200 mg sion, pruritus, injection site discomfort.
twice daily. WEIGHING 30–49 KG: Initially,
1 mg/kg/dose twice daily. May increase ADVERSE EFFECTS/TOXIC
by 1 mg/kg/dose twice daily at wkly inter- REACTIONS
vals. Maintenance: 2–4 mg/kg/dose twice Increased risk of suicidal ideation, be-
daily. WEIGHING 11–29 KG: Initially, 1 mg/kg/ havior. Dose-dependent prolongations in
dose twice daily. May increase by 1 mg/kg/ PR interval noted. Leukopenia, anemia,
dose twice daily at wkly intervals. Mainte- thrombocytopenia occur rarely.
nance: 3–6 mg/kg/dose twice daily.
Adjunctive Therapy NURSING CONSIDERATIONS
PO/IV: ADULTS, ELDERLY: Initially, 50 mg BASELINE ASSESSMENT
twice daily. May increase by 50 mg twice daily Review history of seizure disorder (in-
at wkly intervals. Maintenance: 100–200 tensity, frequency, duration, level of
mg twice daily. Maximum: 400 mg/ consciousness). Initiate seizure precau-
day. CHILDREN 4–17 YRS, WEIGHING 50 KG OR tions. Renal function, LFT, CBC should
MORE: Initially, 50 mg twice daily. Main-
be performed before therapy begins and
tenance: 100–200 mg twice daily. WEIGH- periodically during therapy. Question
ING 30–49 KG: Initially, 1 mg/kg/dose twice
history of cardiac conduction disor-
daily. Maintenance: 2–4 mg/kg/dose twice ders, depression, suicidal ideation and
daily. WEIGHING 11–29 KG: Initially, 1 mg/kg/ behavior.
dose twice daily. Maintenance: 3–6 mg/
kg/dose twice daily. INTERVENTION/EVALUATION
Observe for recurrence of seizure ac-
Switch from IV to PO
tivity. Assess for clinical improvement
When switching from IV to PO form, use (decrease in intensity/frequency of sei-
same equivalent daily dosage and fre- zures). Assist with ambulation if dizzi-
quency as IV administration. ness occurs. Assess for suicidal ideation,
Switch from PO to IV depression, behavioral changes. Drug
When switching from PO to IV form, initial should be withdrawn gradually (over a
total daily IV dosage should be equivalent to minimum of 1 wk) to minimize potential
total daily dosage and frequency of PO form for increased seizure frequency. Monitor
and should be infused IV over 30–60 min. ECG for QT prolongation.

underlined – top prescribed drug


lactulose 657
PATIENT/FAMILY TEACHING LIFESPAN CONSIDERATIONS
• Strict maintenance of drug therapy is Pregnancy/Lactation: Unknown if
essential for seizure control. • Avoid drug crosses placenta or is distributed
tasks that require alertness, motor skills in breast milk. Children: Avoid use in
until response to drug is established. pts younger than 6 yrs (usually unable to
• Avoid alcohol. • Report depression, describe symptoms). Elderly: No age-
suicidal ideation, unusual behavioral related precautions noted.
changes.
INTERACTIONS
DRUG: None significant. HERBAL: None
significant. FOOD: None known. LAB
lactulose VALUES: May decrease serum potassium
(GI loss).
lak-tyoo-lose
(Apo-Lactulose , Constulose, AVAILABILITY (Rx)
Enulose, Generlac, Kristalose) Packets: (Kristalose): 10 g, 20 g. Solu-
Do not confuse lactulose with tion, Oral: 10 g/15 mL.
lactose.
ADMINISTRATION/HANDLING
uCLASSIFICATION L
PO
PHARMACOTHERAPEUTIC: Lactose • Store solution at room tempera-
derivative. CLINICAL: Hyperosmotic ture. • Solution appears pale yellow to
laxative, ammonia detoxicant. yellow, viscous liquid. Cloudiness, dark-
ened solution does not indicate potency
USES loss. • Drink water, juice, milk with each
dose (aids stool softening, increases palat-
Prevention, treatment of portal-systemic ability). • Mix packets with 4 oz water.
encephalopathy (including hepatic pre-
coma, coma); treatment of constipation. Rectal
• Lubricate anus with petroleum jelly
PRECAUTIONS before enema insertion. • Insert care-
Contraindications: Hypersensitivity to fully (prevents damage to rectal wall)
lactulose. Pts requiring a low-galactose with nozzle toward navel. • Squeeze
diet. Cautions: Diabetes, hepatic impair- container until entire dose ex-
ment, dehydration. pelled. • Instruct pt to retain 30–60
min in divided doses. • Maximum: 60
ACTION mL/day (40 g/day).
Inhibits diffusion of NH3 into blood by
converting NH3 to NH4+; enhances diffu- INDICATIONS/ROUTES/DOSAGE
sion of NH3 from blood to gut, where it Constipation
is converted to NH4+; produces osmotic PO: ADULTS, ELDERLY: 15–30 mL (10–20
effect in colon, resulting in colon disten- g)/day, up to 60 mL (40 g)/day. CHIL-
tion, promoting peristalsis. Therapeutic DREN: 1.5–3 mL/kg/day (1–2 g/kg/day) in
Effect: Promotes increased peristalsis, 1–2 divided doses. Maximum: 60 mL/day.
bowel evacuation; decreases serum am-
monia concentration. Prevention of Portal-Systemic
Encephalopathy
PHARMACOKINETICS ADULTS, ELDERLY:30–45 mL (20–30 g)
Poorly absorbed from GI tract. Exten- 3–4 times/day. Adjust dose q1–2 days
sively metabolized in colon. Primarily to produce 2–3 soft stools/day. CHIL-
excreted in feces. DREN: 40–90 mL/day (26.7–60 g/day)

Canadian trade name Non-Crushable Drug High Alert drug


658 lamivudine/­tenofovir
in divided doses 3–4 times/day. IN- pts for symptom improvement (alertness,
FANTS: 2.5–10 mL/day (1.7–6.7 g/day) orientation, ability to follow commands).
in 3–4 divided doses. Adjust dose q1–2
PATIENT/FAMILY TEACHING
days to produce 2–3 soft stools/day.
• Evacuation occurs in 24–48 hrs of initial
Treatment of Portal-Systemic dose. • Institute measures to promote
Encephalopathy defecation: increase fluid intake, exercise,
PO: ADULTS, ELDERLY: Initially, 30–45 mL high-fiber diet. • Drink plenty of flu-
(20–30 g) every hr to induce rapid laxation. ids. • If therapy was started to treat high
Then, 30–45 mL 3–4 times/day. Adjust dose ammonia levels, notify physician if worsen-
q1–2days to produce 2–3 soft stools/day. ing of confusion, lethargy, weakness occurs.
Rectal Administration (as Retention
Enema) lamivudine/­
200 g (300 mL) diluted with 700 mL water
or NaCl via rectal balloon catheter. Retain tenofovir
30–60 min q4–6h. (Transition to oral
prior to stopping rectal administration.) la-miv-ue-deen/ten-oh-foe-veer
(Cimduo)
Dosage in Renal/Hepatic Impairment j BLACK BOX ALERT j Severe
L No dose adjustment. exacerbations of hepatitis B virus
(HBV) reported in pts co-infected
SIDE EFFECTS with HIV-1 and HBV following
discontinuation. If discontinuation
Occasional: Abdominal cramping, flatu- occurs, monitor hepatic function for
lence, increased thirst, abdominal dis- at least several mos. Initiate anti-
comfort. Rare: Nausea, vomiting. HBV therapy if warranted.
Do not confuse lamivudine/teno-
ADVERSE EFFECTS/TOXIC fovir (Cimduo) with lamivudine/
REACTIONS nevirapine/zidovudine, efavirenz/
Severe diarrhea may cause dehydration, emtricitabine/tenofovir (Atripla),
electrolyte imbalance. Long-term use may efavirenz/lamivudine/tenofovir
result in laxative dependence, chronic con- (Symfi Lo) abacavir/dolutegravir/
stipation, loss of normal bowel function. lamivudine (Triumeq), abacavir/
lamivudine/zidovudine (Trizivir),
NURSING CONSIDERATIONS bictegravir/emtricitabine/tenofo-
vir (Biktarvy).
BASELINE ASSESSMENT
Question usual stool pattern, frequency, FIXED-COMBINATION(S)
characteristics. Conduct neurological Cimduo: lamivudine/tenofovir (antiret-
exam in pts with elevated serum ammo- rovirals): 300 mg/300 mg.
nia levels, symptoms of encephalopathy.
uCLASSIFICATION
Assess hydration status.
PHARMACOTHERAPEUTIC: Nucleo-
INTERVENTION/EVALUATION side reverse transcriptase inhibitor,
Encourage adequate fluid intake. As- nucleotide reverse transcriptase
sess bowel sounds for peristalsis. Moni- inhibitor. CLINICAL: Antiretroviral
tor daily pattern of bowel activity, stool agent (anti-HIV).
consistency; record time of evacuation.
Assess for abdominal disturbances. USES
Monitor serum electrolytes in pts with Treatment of HIV-1 infection in adult and pe-
prolonged, frequent, excessive use of diatric pts weighing at least 35 kg, in combi-
medication. Monitor encephalopathic nation with other antiretroviral agents.
underlined – top prescribed drug
lamivudine/­tenofovir 659

PRECAUTIONS known. LAB VALUES: May increase serum


Contraindications: Hypersensitivity to la- amylase, ALT, AST, creatine kinase (CK),
mivudine, tenofovir. Cautions: Hepatic/ cholesterol, glucose, triglycerides. May de-
renal impairment, hyperlipidemia, psy- crease neutrophils.
chiatric illness (e.g., depression); history
AVAILABILITY (Rx)
of pathological fracture, osteoporosis,
osteopenia. History of pancreatitis (pedi- Fixed-Dose Combination Tablets: lamivu-
atric pts). Not recommended in pts with dine/tenofovir: 300 mg/300 mg.
CrCl less than 50 mL/min, end-stage renal
ADMINISTRATION/HANDLING
disease requiring hemodialysis.
PO
ACTION • Give without regard to food.
Lamivudine inhibits HIV reverse transcrip-
INDICATIONS/ROUTES/DOSAGE
tion via viral DNA chain termination; inhib-
its RNA- and DNA-dependent polymerase HIV-1 Infection
activities. Tenofovir interferes with HIV viral PO: ADULTS, CHILDREN WEIGHING AT
RNA-dependent DNA polymerase. Thera- LEAST 35 KG: 1 tablet once daily (in com-
peutic Effect: Inhibits viral replication, bination with other antiretrovirals).
slowing progression of HIV infection. Dosage in Renal Impairment L
CrCl greater than 50 mL/min: No dose
PHARMACOKINETICS
adjustment. CrCl less than 50 mL/min,
Widely distributed. Tenofovir metabolized ESRD requiring HD: Not recommended.
by enzymatic hydrolysis, mediated by mac-
rophages and hepatocytes. Protein binding: Dosage in Hepatic Impairment
(lamivudine): less than 36%, (tenofovir): Mild to moderate impairment: No
less than 1%. Lamivudine excreted primar- dose adjustment. Severe impairment:
ily in urine. Tenofovir excreted primarily in Not recommended.
urine (70–80%). Half-life: (lamivudine):
5–7 hrs; (tenofovir): 17 hrs. SIDE EFFECTS
Frequent (18%–11%): Rash, urticaria,
LIFESPAN CONSIDERATIONS headache, pain, diarrhea. Occasional (9%–
Pregnancy/Lactation: Breastfeed- 4%): Back pain, nausea, fever, abdominal
ing not recommended due to risk of pain, asthenia, anxiety, insomnia, vomiting,
postnatal HIV transmission. Lamivudine, arthralgia, dyspepsia. Rare (3%–1%): Myal-
tenofovir are secreted in breast milk. gia, dizziness, peripheral neuropathy.
Children: Safety and efficacy not estab-
lished in children weighing less than 35 ADVERSE EFFECTS/TOXIC
kg. May have increased risk of pancreati- REACTIONS
tis. Elderly: May have increased risk of May cause new or worsening renal fail-
adverse reactions/toxic reactions. ure including Fanconi syndrome (renal
tubular injury, nonabsorption of essen-
INTERACTIONS tial electrolytes, acids, buffers in renal
DRUG: Adefovir may decrease thera- tubules). Renal tubular injury may lead
peutic effect/increase concentration of to rhabdomyolysis, osteomalacia, muscle
tenofovir. Tenofovir may decrease weakness, myopathy. May decrease bone
therapeutic effect of didanosine. La- mineral density, leading to pathological
mivudine may increase adverse/toxic fractures. May cause redistribution/ac-
effect of emtricitabine. NSAIDs (e.g., cumulation of body fat (lipodystrophy).
ibuprofen, naproxen, ketorolac) may Fatal lactic acidosis, severe hepato-
increase nephrotoxic effect of tenofovir. megaly with steatosis (fatty liver) were
HERBAL: None significant. FOOD: None reported. If therapy is discontinued, pts
Canadian trade name Non-Crushable Drug High Alert drug
660 lamoTRIgine
co-infected with hepatitis B or C virus greater than 0.4 mg/dL from baseline
have an increased risk for viral replica- may indicate renal impairment. Monitor
tion, worsening of hepatic function, and for immune recovery syndrome, esp. af-
may experience hepatic decompensa- ter initiating treatment. Cough, dyspnea,
tion and/or failure. May induce immune fever, excess band cells on CBC may
recovery syndrome (inflammatory re- indicate acute infection (WBC may be
sponse to dormant opportunistic infec- unreliable in pts with uncontrolled HIV
tions, such as Mycobacterium avium, infection). Monitor daily pattern of bowel
cytomegalovirus, PCP, tuberculosis, or activity, stool consistency; I&Os. Screen
acceleration of autoimmune disorders for depression. Obtain serum amylase, li-
including Graves’ disease, polymyositis, pase level if acute pancreatitis suspected
Guillain-Barré). Fatal cases of pancre- (pediatric pts).
atitis may occur in pediatric pts with
prior use of antiretroviral nucleosides or PATIENT/FAMILY TEACHING
history of pancreatitis. Early virological • Treatment does not cure HIV infection
failure and high rate of resistance substi- nor reduce risk of transmission. Practice
tutions may occur. Depression reported safe sex with barrier methods or absti-
in 11% of pts. Hematuria occurred in 7% nence. • Drug resistance can form if
of pts. treatment is interrupted; do not run out of
L supply. • As immune system strengthens,
NURSING CONSIDERATIONS it may respond to dormant infections hid-
den within the body. Report any new fever,
BASELINE ASSESSMENT
chills, body aches, cough, night sweats,
Obtain, BUN, serum creatinine, CrCl, shortness of breath. • Report symptoms
eGFR, CD4+ count, viral load, HIV-1 RNA of kidney inflammation or disease (de-
level; urine glucose, urine protein; preg- creased urine output, abdominal pain,
nancy test in females of reproductive po- darkened urine); toxic skin reactions
tential. Obtain serum phosphate level in (rash, pustules, skin eruptions). • Pan-
pts with renal impairment. Test all pts for creatitis can occur in children; report any
HBV infection. Receive full ­medication new or worsening abdominal pain that
history and screen for contraindications/ radiates to the back or shoulder, with or
interactions. Question history of he- without nausea/vomiting. • Do not
patic/renal impairment, hyperlipidemia, breastfeed. • Decreased bone density
hypersensitivity reactions, decreased
­ may lead to pathological fractures; report
mineral bone density, osteopenia, de- bone/extremity pain, suspected frac-
pression; pancreatitis (in children). tures. • Antiretrovirals may cause excess
­Offer emotional support. body fat in upper back, neck, breast,
trunk, while also causing decreased body
INTERVENTION/EVALUATION
fat in legs, arms, face. • Do not take
Monitor CD4+ count, viral load, HIV-1 newly prescribed medications, including
RNA level for treatment effectiveness. OTC drugs, unless approved by prescriber
Monitor LFT; assess for hepatic injury who originally started treatment.
(bruising, hematuria, jaundice, right up-
per abdominal pain, nausea, vomiting,
weight loss). If discontinuation of drug
regimen occurs, monitor hepatic func- lamoTRIgine
tion for at least several mos. Initiate anti-
HBV therapy if warranted. Obtain serum la-moe-tri-jeen
lactate level if lactic acidosis suspected. (LaMICtal, LaMICtal ODT, LaMICtal
Monitor renal function as clinically indi- XR, Subvenite)
cated. An increase in serum creatinine

underlined – top prescribed drug


lamoTRIgine 661

j BLACK BOX ALERT jSevere, LIFESPAN CONSIDERATIONS


potentially life-threatening skin
rashes have been reported, including Pregnancy/Lactation: Distributed in
Stevens-Johnson syndrome. Risk breast milk. Breastfeeding not recommended.
increased with coadministration with Increased fetal risk of oral cleft formation has
valproic acid and rapid-dose titration. been noted with use during pregnancy. Chil-
Do not confuse LaMICtal dren: Safety and efficacy not established in
with LamISIL or Lomotil, or pts younger than 18 yrs with bipolar disorder
lamoTRIgine with labetalol or or in pts younger than 13 yrs with epilepsy.
lamiVUDine. Elderly: Age-related renal impairment may
require dosage adjustment.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Phenyl- INTERACTIONS
triazine. CLINICAL: Anticonvulsant. DRUG: CarBAMazepine, PHENobarbi-
tal, primidone, phenytoin, rifAMPin
may decrease concentration/effect. Valproic
USES acid may increase concentration/effects.
Immediate-Release: Adjunctive therapy May increase adverse effects of carBAMaze-
in adults and children 2 yrs of age and older pine, dofetilide. Estrogen (contracep-
with generalized tonic-clonic seizures, par- tive) may decrease concentration/effect. CNS
tial seizures, and generalized seizures of depressants (e.g., alcohol, morphine, L
Lennox-Gastaut syndrome. Conversion to zolpidem) may increase CNS depression.
monotherapy in adults treated with another HERBAL: Herbals with sedative properties
enzyme-inducing antiepileptic drug (EIAED) (e.g., chamomile, kava kava, valerian)
(e.g., valproic acid, carBAMazepine, phe- may increase CNS depression. FOOD: None
nytoin, PHENobarbital, or primidone as known. LAB VALUES: None significant.
the single antiepileptic drug). Long-term
maintenance treatment of bipolar disor- AVAILABILITY (Rx)
der. Treatment of pts 2 yrs and older with Tablets: 25 mg, 100 mg, 150 mg, 200
primary generalized tonic-clonic seizures. mg. Tablets, Chewable: 5 mg, 25 mg.
Extended-Release: Adjunctive therapy Tablets, Orally Disintegrating: 25 mg, 50
for primary generalized tonic-clonic and mg, 100 mg, 200 mg.
partial-onset seizures in pts 13 yrs and older. Tablets, Extended-Release: 25 mg,
Conversion to monotherapy in pt 13 yrs and 50 mg, 100 mg, 200 mg, 250 mg, 300 mg.
older with partial seizures receiving treat-
ment with a single antiepileptic drug (AED). ADMINISTRATION/HANDLING
PO
PRECAUTIONS • Give without regard to food. • Chew-
Contraindications: Hypersensitivity to la- able tablets may be dispensed in water or
moTRIgine. Cautions: Renal/hepatic impair- diluted fruit juice, or swallowed whole.
ment, pts at high risk of suicide, pts taking • Extended-release tablets must be swal-
estrogen-containing oral contraceptives, his- lowed whole; do not break, crush,
tory of adverse hematologic reaction. ­dissolve, or divide. • Place orally disinte-
grating tablet on tongue, allow to dissolve.
ACTION Pt must not break, cut, or chew. Can be
Inhibits voltage-sensitive sodium chan- swallowed without regard to food or water.
nels, stabilizing neuronal membranes. In-
hibits release of glutamide (an excitatory INDICATIONS/ROUTES/DOSAGE
amino acid). Therapeutic Effect: Re- Lennox-Gastaut, Primary Generalized
duces frequency of seizure activity. Delays Tonic-Clonic Seizures, Partial Seizures
time to occurrence of acute mood epi- PO: ADULTS, ELDERLY, CHILDREN OLDER THAN
sodes (mania, depression, hypomania). 12 YRS: Initially, 25 mg/day for 2 wks, then
Canadian trade name Non-Crushable Drug High Alert drug
662 lamoTRIgine
increase to 50 mg/day for 2 wks. After 4 wks, Usual Maintenance Range for Extended-
may increase by 50 mg/day at 1- to 2-wk in- Release Tablets
tervals. Maintenance: 225–375 mg/day in PT TAKING VALPROIC ACID: 200–250 mg
2 divided doses. CHILDREN 2–12 YRS: Note: once daily. PT TAKING EIAED WITHOUT VAL-
Only whole tablets should be used for dos- PROIC ACID: 400–600 mg once daily. PT
ing. Round dose down to nearest whole NOT TAKING EIAED: 300–400 mg once daily.
tablet. Initially, 0.3 mg/kg/day in 1–2 divided Conversion to Monotherapy for Pts
doses for 2 wks, then increase to 0.6 mg/kg/ Receiving EIAEDs
day in 1–2 divided doses for 2 wks. After 4 PO: ADULTS, ELDERLY, CHILDREN 16 YRS AND
wks, may increase by 0.6 mg/kg/day at 1- to OLDER: 500 mg/day in 2 divided doses.
2-wk intervals. Maintenance: 4.5–7.5 mg/ Titrate to desired dose while maintaining
kg/day in 2 divided doses. Maximum: 300 EIAED at fixed level, then withdraw EIAED
mg/day in 2 divided doses. by 20% each wk over a 4-wk period.
Adjusted Dosage with Antiepileptic Drugs Conversion to Monotherapy for Pts
Containing Valproic Acid Receiving Valproic Acid
PO: ADULTS, ELDERLY, CHILDREN OLDER PO: ADULTS, ELDERLY, CHILDREN 16 YRS
THAN 12 YRS: Initially, 12.5–25 mg every AND OLDER: Titrate lamoTRIgine to 200
other day for 2 wks, then increase to 25 mg/ mg/day, maintaining valproic acid dose.
L day for 2 wks. After 4 wks, may increase Maintain lamoTRIgine dose and decrease
by 25–50 mg/day at 1- to 2-wk intervals. valproic acid to 500 mg/day, no greater
Maintenance: 100–400 mg/day in 2 di- than 500 mg/day, then maintain 500 mg/
vided doses (100–200 mg/day when taking day for 1 wk. Increase lamoTRIgine to
lamoTRIgine with valproic acid alone). CHIL- 300 mg/day and decrease valproic acid
DREN 2–12 YRS: Note: Only whole tablets to 250 mg/day. Maintain for 1 wk, then
should be used for dosing. Round dose down discontinue valproic acid and increase
to nearest whole tablet. Initially, 0.15 mg/kg/ lamoTRIgine by 100 mg/day each wk until
day in 1–2 divided doses for 2 wks, then in- maintenance dose of 500 mg/day reached.
crease to 0.3 mg/kg/day in 1–2 divided doses
for 2 wks. After 4 wks, may increase by 0.3 Bipolar Disorder
mg/kg/day at 1- to 2-wk intervals. Mainte- PO: ADULTS, ELDERLY: Initially, 25 mg/
nance: 1–5 mg/kg/day in 2 divided doses. day for 2 wks, then 50 mg/day for 2 wks,
Maximum: 200 mg/day in 2 divided doses. then 100 mg/day for 1 wk, then 200 mg/
day beginning with wk 6.
Adjusted Dosage with EIAED without
Valproic Acid Bipolar Disorder in Pts Receiving EIAEDs
PO: ADULTS, ELDERLY, CHILDREN OLDER PO: ADULTS, ELDERLY: 50 mg/day for 2
THAN 12 YRS: Initially, 50 mg/day for 2 wks, wks, then 100 mg/day for 2 wks, then
then increase to 100 mg/day in 2 divided 200 mg/day for 1 wk, then 300 mg/day
doses for 2 wks. After 4 wks, may increase for 1 wk, then up to usual maintenance
by 100 mg/day at 1- to 2-wk intervals. dose 400 mg/day in divided doses.
Maintenance: 300–500 mg/day in 2 Bipolar Disorder in Pts Receiving Valproic
divided doses. CHILDREN 2–12 YRS: Note: Acid
Only whole tablets should be used for dos- PO: ADULTS, ELDERLY: 25 mg/day every
ing. Round dose down to nearest whole tab- other day for 2 wks, then 25 mg/day for 2
let. Initially, 0.6 mg/kg/day in 1–2 divided wks, then 50 mg/day for 1 wk, then 100
doses for 2 wks, then increase to 1.2 mg/ mg/day. Usual maintenance dose with
kg/day in 1–2 divided doses for 2 wks. After valproic acid: 100 mg/day.
4 wks, may increase by 1.2 mg/kg/day at
1- to 2-wk intervals. Maintenance: 5–15 Usual Dosage for LaMICtal XR
mg/kg/day in 2 divided doses. Maxi- Adjunct therapy: Range: 200–600
mum: 400 mg/day in 2 divided doses. mg/day.
underlined – top prescribed drug
lansoprazole 663
Conversion to monotherapy: Range: medication history (esp. other anticonvul-
250–500 mg/day. sants), other medical conditions (e.g., renal
impairment). Initiate seizure precautions.
Discontinuation Therapy Assess baseline mood, behavior. Question
b ALERT c A dosage reduction of ap- history of suicidal thought and behavior.
proximately 50%/wk over at least 2 wks
is recommended. INTERVENTION/EVALUATION
Report occurrence of rash (drug discon-
Dosage in Renal Impairment tinuation may be necessary). Assist with
b ALERT c Decreased dosage may be ambulation if dizziness, ataxia occurs. As-
effective in pts with significant renal im- sess for clinical improvement (decreased
pairment. intensity/frequency of seizures). Assess
for visual abnormalities, headache. Mon-
Dosage in Hepatic Impairment
itor for suicidal ideation, depression, be-
Mild impairment: No dose adjustment.
havioral changes.
Moderate to severe impairment with-
out ascites: Reduce dose by 25%. Se- PATIENT/ FAMILY TEACHING
vere impairment with ascites: Reduce • Take medication only as prescribed;
dose by 50%. do not abruptly discontinue medication
after long-term therapy. • Avoid alco- L
SIDE EFFECTS hol. • Avoid tasks that require alert-
Frequent (38%–14%): Dizziness, head- ness, motor skills until response to drug
ache, diplopia, ataxia, nausea, blurred is established. • Carry identification
vision, drowsiness, rhinitis. Occasional card/bracelet to note anticonvulsant
(10%–5%): Rash, pharyngitis, vomiting, therapy. • Strict maintenance of drug
cough, flu-like symptoms, diarrhea, dys- therapy is essential for seizure con-
menorrhea, fever, insomnia, dyspepsia. trol. • Report any rash, fever, swelling
Rare: Constipation, tremor, anxiety, pru- of glands, worsening depression, suicidal
ritus, vaginitis, hypersensitivity reaction. ideation, unusual changes in behavior,
worsening of seizure control. • May
ADVERSE EFFECTS/TOXIC cause photosensitivity reaction; avoid ex-
REACTIONS posure to sunlight, ultraviolet light.
Abrupt withdrawal may increase seizure
frequency. Serious rashes, including
Stevens-Johnson syndrome, have been
reported. May increase risk of suicidal
thoughts and behavior. Hemophagocytic lansoprazole
lymphohistiocytosis, a life-threatening
syndrome of extreme systemic inflamma- lan-soe-pra-zole
tion characterized by hepatosplenomeg- (Prevacid, Prevacid Solu-Tab,
aly, lymphadenopathy, fever, rash, organ Prevacid 24HR)
dysfunction, has occurred. Life-threaten- Do not confuse lansoprazole
ing eosinophilia and systemic symptoms with ARIPiprazole or dexlanso-
(DRESS) may occur. May increase risk prazole, or Prevacid with Pra-
of aseptic meningitis. Abrupt withdrawal vachol, PriLOSEC, or Prinivil.
may increase frequency of seizures. FIXED-COMBINATION(S)
NURSING CONSIDERATIONS Prevacid NapraPac: lansoprazole/
naproxen (an NSAID): 15 mg/375
BASELINE ASSESSMENT mg, 15 mg/500 mg. Prevpac: Com-
Review history of seizure disorder (type, bination card containing amoxicillin
onset, intensity, frequency, duration, LOC), 500 mg (4 capsules), lansoprazole 30

Canadian trade name Non-Crushable Drug High Alert drug


664 lansoprazole
mg (2 capsules), clarithromycin 500 Half-life: 1.5 hrs (increased in hepatic
mg (2 tablets). impairment, elderly).
uCLASSIFICATION LIFESPAN CONSIDERATIONS
PHARMACOTHERAPEUTIC: Proton Pregnancy/Lactation: Unknown if dis­
pump inhibitor. CLINICAL: Anti- tributed in breast milk. Children: Safety
ulcer agent. and efficacy not established. Elderly: No
age-related precautions not­ed but doses
USES greater than 30 mg not recommended.
Short-term treatment (4 wks and less) of
healing, symptomatic relief of active duo- INTERACTIONS
denal ulcer; short-term treatment (8 wks DRUG: May decrease concentration/ef-
and less) for healing, symptomatic relief of fect of atazanavir. May increase effect of
erosive esophagitis. Long-term treatment of warfarin. May decrease effect of clopi-
pathologic hypersecretory conditions, in- dogrel, risedronate. May decrease
cluding Zollinger-Ellison syndrome. Short- concentration/effects of acalabrutinib,
term treatment (8 wks and less) of active cefuroxime, erlotinib, neratinib,
benign gastric ulcer, H. pylori–associated pazopanib. Strong CYP2C19 induc-
duodenal ulcer (part of multidrug regi- ers (e.g., fluoxetine), strong CYP3A4
L men), maintenance treatment for healed inducers (e.g., carBAMazepine,
duodenal ulcer. Treatment of gastro- phenytoin, rifAMPin) may decrease
esophageal reflux disease (GERD), NSAID- concentration/effect. HERBAL: St. John’s
associated gastric ulcer. Reduce risk of wort may decrease concentration/effect.
NSAID-associated gastric ulcer in pts with FOOD: Food may decrease absorption.
history of gastric ulcer requiring NSAIDs. LAB VALUES: May increase serum LDH,
OTC: Relief of frequent heartburn (2 or alkaline phosphatase, bilirubin, choles-
more days/wk). IV: Short-term treatment terol, creatinine, ALT, AST, triglycerides,
of erosive esophagitis. OFF-LABEL: Stress uric acid; Hgb, Hct. May produce abnor-
ulcer prophylaxis in critically ill. mal albumin/globulin ratio, electrolyte
balance, platelet, RBC, WBC count.
PRECAUTIONS
Contraindications: Hypersensitivity to AVAILABILITY (Rx)
lan­soprazole, other proton pump in- Tablets, Orally Disintegrating: 15 mg, 30
hibitors. Concomitant use with rilpiv- mg.
irine. Cautions: Hepatic impairment. Capsules, Delayed-Release: 15 mg, 30
May increase risk of hip, wrist, spine mg.
fractures; GI infections.
ADMINISTRATION/HANDLING
ACTION PO
Inhibits the (H+, K+)–ATPase enzyme sys- • Best if taken before breakfast • Do not
tem, blocking the final step in gastric acid cut/crush delayed-release capsules. • If
secretion. Therapeutic Effect: Sup- pt has difficulty swallowing capsules, open
presses gastric acid secretion. capsules, sprinkle granules on 1 tbsp of
applesauce, give immediately. Do not crush
PHARMACOKINETICS or allow pt to chew granules.
Rapid, complete absorption (food may
decrease absorption) once drug has left PO (Solu-Tab)
stomach. Protein binding: 97%. Distrib- • Place tablet on tongue; allow to dissolve,
uted primarily to gastric parietal cells. then swallow. • May give via oral syringe
Metabolized in liver. Excreted in bile or nasogastric tube. • May dissolve in 4
and urine. Not removed by hemodialysis. mL (15 mg) or 10 mL (30 mg) water.

underlined – top prescribed drug


lapatinib 665

INDICATIONS/ROUTES/DOSAGE SIDE EFFECTS


Duodenal Ulcer Occasional (3%–2%): Diarrhea, abdomi-
PO: ADULTS, ELDERLY:15 mg/day, for up nal pain, rash, pruritus, altered appetite.
to 4 wks. Maintenance: 15 mg/day. Rare (1%): Nausea, headache.

Erosive Esophagitis ADVERSE EFFECTS/TOXIC


PO: ADULTS, ELDERLY: 30 mg/day, for up REACTIONS
to 8 wks. If healing does not occur within Bilirubinemia, eosinophilia, hyperlipid-
8 wks may give for additional 8 wks. emia occur rarely. May increase risk of
Maintenance: 15 mg/day. CHILDREN C. difficile infection. Chronic use may
1–11 YRS, WEIGHING MORE THAN 30 KG: 30 increase risk of osteoporosis, fractures.
mg/day for up to 12 wks; WEIGHING 30 KG
OR LESS: 15 mg/day for up to 12 wks. NURSING CONSIDERATIONS
Gastric Ulcer BASELINE ASSESSMENT
PO: ADULTS: 30 mg/day for up to 8 wks. Obtain baseline lab values. Assess for
NSAID Gastric Ulcer epigastric/abdominal pain, evidence of
PO: ADULTS, ELDERLY: Healing: 30 mg/ GI bleeding, ecchymosis.
day for up to 8 wks. Prevention: 15 mg/ INTERVENTION/EVALUATION
day for up to 12 wks. L
Monitor CBC, hepatic/renal function tests.
Gastroesophageal Reflux Disease (GERD) Assess for therapeutic response (relief of
PO: ADULTS: 15 mg/day for up to 8 wks. GI symptoms). Question if diarrhea, ab-
CHILDREN 12–17 YRS: 30 mg/day up to 8 dominal pain, nausea occurs. Obtain C.
wks. CHILDREN 1–11 YRS, WEIGHING MORE difficile PCR test in pts with persistent
THAN 30 KG: 30 mg/day for up to 8 wks; diarrhea, fever, abdominal pain.
WEIGHING 30 KG OR LESS: 15 mg/day for
PATIENT/ FAMILY TEACHING
up to 8 wks.
• Do not chew, crush delayed-release
H. Pylori Infection capsules. • For pts who have difficulty
PO: ADULTS, ELDERLY: (triple drug therapy swallowing capsules, open capsules,
including amoxicillin, clarithromycin) 30 sprinkle granules on 1 tbsp of applesauce,
mg q12h for 10–14 days or (with amoxicil- swallow immediately.
lin) 30 mg 3 times/day for 14 days.
Pathologic Hypersecretory Conditions
(Including Zollinger-Ellison Syndrome)
lapatinib
PO: ADULTS, ELDERLY: Initially, 60 mg/
la-pa-tin-ib
day. Individualize dosage according to pt (Tykerb)
needs and for as long as clinically indi-
cated. Administer doses greater than 120 j BLACK BOX ALERT jHepatotox-
icity (serum ALT or AST more than
mg/day in divided doses. 3 times upper limit of normal [ULN]
and total bilirubin more than 2 times
Heartburn (OTC) ULN), possibly severe, has occurred.
PO: ADULTS, ELDERLY: 15 mg once daily Do not confuse lapatinib with
for 14 days. May repeat q4mos. dasatinib, erlotinib, or imatinib.
Dosage in Renal Impairment
uCLASSIFICATION
No dose adjustment.
PHARMACOTHERAPEUTIC: Epider-
Dosage in Hepatic Impairment mal growth factor receptor (EGFR)
Consider dose reduction in severe inhibitor. Tyrosine kinase inhibitor.
impairment. CLINICAL: Antineoplastic.

Canadian trade name Non-Crushable Drug High Alert drug


666 lapatinib

USES milk. Children: Safety and efficacy not


Combination treatment with capecitabine established. Elderly: No age-related
for the treatment of human epidermal precautions noted.
growth receptor type 2 (HER2)–overex-
INTERACTIONS
pressing advanced or metastatic breast
cancer in pts who have received prior DRUG: QT interval–prolonging
therapy including an anthracycline, a medi­ cations (e.g., amiodarone,
taxane, and trastuzumab. Combination azithromycin, ceritinib, haloperi-
treatment with letrozole for treatment dol, moxi­floxacin) may increase risk
of postmenopausal women with HER2- of QT interval prolongation, cardiac ar-
overexpressing hormone receptor–posi- rhythmias. CYP3A4 inhibitors (e.g.,
tive metastatic breast cancer for whom clarithromycin, ketoconazole, rito-
hormonal therapy is indicated. OFF- navir), dexamethasone may increase
LABEL: Treatment (in combination with concentration/effect. CYP3A4 inducers
trastuzumab) of HER2-overexpressing (e.g., carBAMazepine, phenytoin, ri-
metastatic breast cancer that progressed fAMPin) may decrease concentration/ef-
on prior trastuzumab-containing therapy. fect. HERBAL: St. John’s wort decreases
Treatment of HER2-overexpressing meta- concentration/effect. FOOD: Grapefruit
static breast cancer with brain metastasis. products may increase concentration/
L effect. (potential for torsades, myelotox-
PRECAUTIONS icity). LAB VALUES: May increase serum
Contraindications: Hypersensitivity to ALT, AST, bilirubin. May decrease neutro-
lapatinib. Cautions: Left ventricular func- phils, Hgb, platelets.
tion abnormalities, prolonged QT inter- AVAILABILITY (Rx)
val or medications known to prolong QT
interval, hepatic impairment. History of Tablets: 250 mg.
treatment with anthracyclines, chest wall
irradiation. Avoid concurrent use with ADMINISTRATION/HANDLING
strong CYP3A4 inhibitors or inducers. PO
• Do not break, crush, dissolve, or di-
ACTION vide film-coated tablets. • Give at least
Inhibitory action against kinases target- 1 hr before or 1 hr after food. Take full
ing intracellular components of epidermal dose at same time each day.
growth factor receptor ErbB1 and a second
INDICATIONS/ROUTES/DOSAGE
receptor, human epidermal receptor (HER2
[ErbB2]). Therapeutic Effect: Inhibits Breast Cancer
tumor cell growth and metastasis. PO: ADULTS, ELDERLY: With capecita­
bine: 1,250 mg (5 tablets) once daily.
PHARMACOKINETICS With letrozole: 1,500 mg once daily
Route Onset Peak Duration continuously with letrozole. Continue until
PO 30 min 4 hrs — disease progresses or unacceptable toxicity.
Steady-state level reached within 6–7 days. Dose Modification
Incomplete and variable oral absorption. Cardiac Toxicity
Undergoes extensive metabolism. Protein Discontinue with decreased left ventricu-
binding: 99%. Minimally excreted in feces lar ejection fraction Grade 2 or higher, or
and plasma. Half-life: 24 hrs. in pts with an ejection fraction that drops
to lower limit of normal. May be started at
LIFESPAN CONSIDERATIONS a reduced dose (1,000 mg/day) at a min-
Pregnancy/Lactation: May cause fetal imum of 2 wks when ejection fraction re-
harm. Unknown if distributed in breast turns to normal and pt is asymptomatic.

underlined – top prescribed drug


larotrectinib 667
Pulmonary Toxicity activity, stool consistency. Monitor CBC
Discontinue with symptoms indicative of (particularly Hgb, platelets, neutrophil
interstitial lung disease or pneumonitis count), LFT. Assess hands and feet for
Grade 3 or higher. erythema/blistering/peeling. Monitor
Severe Hepatic Impairment for shortness of breath, palpitations, fa-
With capecitabine: 750 mg/day. With tigue (decreased cardiac ejection frac-
letrozole: 1,000 mg/day. tion). Monitor ECG for QT prolongation.
CYP3A4 Inhibitors/Inducers Obtain CXR if pneumonitis suspected.
Concomitant use of CYP3A4 inhibi-
tors may require dose reduction of PATIENT/FAMILY TEACHING
lapatinib (e.g., decrease to 500 mg/ • Avoid crowds, those with known infec-
day with careful monitoring); CYP3A4 tion. • Avoid contact with those who re-
inducers may require dose increase of cently received live virus vaccine. • Do
lapatinib (e.g., increase to 4,500 mg not have immunizations without physi-
with capecitabine or 5,500 mg with cian’s approval (drug lowers resis-
letrozole). tance). • Promptly report fever, unusual
bruising/bleeding from any site. • En-
Dosage in Renal Impairment
sure use of appropriate birth control mea-
No dose adjustment. sures in women. • Treatment may cause
Dosage in Hepatic Impairment severe lung inflammation; report short- L
Mild to moderate impairment: No ness of breath, severe cough, lung
dose adjustment. Severe impairment: pain. • Report liver problems such as
See dose modification. upper abdominal pain, bleeding, dark or
amber-colored urine, nausea, vomiting,
SIDE EFFECTS or yellowing of the skin or eyes.
Common (65%–44%): Diarrhea, hand-foot
syndrome (blistering/rash/peeling of
skin on palms of hands, soles of feet),
nausea. Frequent (28%–26%): Rash, vom- larotrectinib
iting. Occasional (15%–10%): Mucosal
inflammation, stomatitis, extremity pain, lar-oh-trek-ti-nib
back pain, dry skin, insomnia. (Vitrakvi)
Do not confuse larotrectinib
ADVERSE EFFECTS/TOXIC with alectinib, lapatinib, len-
REACTIONS vatinib, or lorlatinib.
Decreases in left ventricular ejection
Grade 3 or higher have been observed; uCLASSIFICATION
20% decrease relative to baseline is con- PHARMACOTHERAPEUTIC: Tropomy-
sidered toxic. osin receptor kinase (TRK) inhibitor.
Tyrosine kinase inhibitor. CLINICAL:
NURSING CONSIDERATIONS Antineoplastic.
BASELINE ASSESSMENT
Screen for home medications that prolong USES
QT interval. Obtain baseline ECG. Ques- Treatment of adult and pediatric pts with
tion for possibility of pregnancy. Obtain solid tumors that have a neurotrophic
baseline CBC, serum chemistries before receptor tyrosine kinase (NTRK) gene
treatment begins and monthly thereafter. fusion without a known acquired resis-
INTERVENTION/EVALUATION tance mutation; are metastatic or where
Offer antiemetics to control nausea, surgical resection is likely to result in se-
vomiting. Monitor daily pattern of bowel vere morbidity; and have no satisfactory

Canadian trade name Non-Crushable Drug High Alert drug


668 larotrectinib
alternative treatment or that have pro- products may increase concentration/
gressed following treatment. effect. LAB VALUES: May increase serum
alkaline phosphatase, ALT, AST. May de-
PRECAUTIONS crease serum albumin; Hgb, neutrophils,
Contraindications: Hypersensitivity to RBCs.
larotrectinib. Cautions: Baseline anemia,
neutropenia; hepatic impairment, active AVAILABILITY (Rx)
infection, conditions predisposing to in- Capsules: 25 mg, 100 mg. Solution, Oral:
fection (e.g., diabetes, renal failure, im- 20 mg/mL.
munocompromised pts, open wounds);
concomitant use of strong CYP3A inhibi- ADMINISTRATION/HANDLING
tors, strong CYP3A inducers. PO
• Give without regard to food. • Cap-
ACTION sules/oral solution may be used inter-
Inhibits activation of tropomyosin recep- changeably. • If vomiting occurs after
tor kinase (TRK) proteins resulting from administration, give next dose at regu-
NTRK gene fusions, deletion of protein larly scheduled time. • Do not give a
regulatory domain, or in cells with over- missed dose within 6 hrs of next dose.
expression of TRK proteins. Therapeutic Capsules: Administer capsules whole
L Effect: Inhibits tumor cell proliferation with water; do not break, cut, or
and survival. open. • Capsules cannot be chewed.
Solution, Oral: Refrigerate glass bottle. Do
PHARMACOKINETICS not freeze. • Discard unused contents
Widely distributed. Metabolized in liver. after 90 days of first opening bot-
Protein binding: 70%. Excreted in feces tle. • See manufacturer guidelines re-
(58%), urine (39%). Half-life: 2.9 hrs. garding preparation and administration
of oral solution.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Avoid preg- INDICATIONS/ROUTES/DOSAGE
nancy; may cause fetal harm. Female Solid Tumors
pts and male pts with female partners PO: ADULTS, CHILDREN WITH BODY SURFACE
of reproductive potential must use ef- AREA OF AT LEAST 1 m2: 100 mg twice daily.
fective contraception during treatment Continue until disease progression or un-
and for at least 1 wk after discontinua- acceptable toxicity. CHILDREN WITH BODY
tion. Unknown if distributed in breast SURFACE AREA LESS THAN 1 m2: 100 mg/m2
milk. Breastfeeding not recommended twice daily.
during treatment and for at least 1 wk
after discontinuation. May impair fertil- Dose Reduction Schedule
ity. Children: May have increased risk of
increased weight, neutropenia. Elderly: Dose Adults/ Children with
Not specified; use caution. Reduction Children with Body Surface
for Adverse Body Surface Area Less
INTERACTIONS Reactions Area of at Than 1 m2
DRUG: Strong CYP3A4 inhibitors Least 1 m2
(e.g., clarithromycin, ketoconazole) First 75 mg twice 75 mg/m2
may increase concentration/effect. daily twice daily
Strong CYP3A4 inducers (e.g., car- Second 50 mg twice 50 mg/m2
BAMazepine, phenytoin, rifAMPin) daily twice daily
may decrease concentration/effect. Third 100 mg once 25 mg/m2
HERBAL: St. John’s wort may decrease daily twice daily
concentration/effect. FOOD: Grapefruit
underlined – top prescribed drug
larotrectinib 669
Dose Modification cluding delirium (2% of pts), dysarthria
Based on Common Terminology Criteria (1% of pts), dizziness (1% of pts), gait
for Adverse Events (CTCAE). disturbance (1% of pts), memory im-
pairment (1% of pts), paresthesia (1% of
Any Grade 3 or 4 Adverse Reaction pts), tremor (1% of pts) occurred in
Note (includes hepatotoxicity and neu- 53% of pts. Grade 4 encephalopathy re-
rotoxicity): Withhold treatment until ported in less than 1% of pts. Hepatotox-
resolved or improved to Grade 1, then icity with transaminase elevations of any
resume at next lower dose level. If not grade reported in 45%. Grade 3 hepato-
resolved within 4 wks, permanently toxicity reported in 6% of pts. Falls re-
discontinue. ported in 10% of pts.
Concomitant Use of Strong CYP3A4 NURSING CONSIDERATIONS
Inhibitor
If strong CYP3A4 inhibitor cannot be BASELINE ASSESSMENT
discontinued, reduce larotrectinib dose Obtain CBC, LFTs; pregnancy test in fe-
by 50%. If strong CYP3A inhibitor is dis- males of reproductive potential. Confirm
continued for 3–5 half-lives, resume presence of NTRK gene fusion in tumor
larotrectinib dose prior to use of strong specimen. Screen for active infection.
CYP3A4 inhibitor. Confirm compliance of effective contra- L
ception. Question history of hepatic im-
Concomitant Use of Strong CYP3A4 pairment. Receive full medication history
Inducer and screen for interactions. Initiate fall
If strong CYP3A4 inducer cannot be dis- precautions. Offer emotional support.
continued, double the larotrectinib dose. If
strong CYP3A inducer is discontinued for INTERVENTION/EVALUATION
3–5 half-lives, resume larotrectinib dose Monitor CBC for anemia, neutropenia
prior to use of strong CYP3A4 inducer. periodically; LFTs for hepatotoxicity
(bruising, hematuria, jaundice, right up-
Dosage in Renal Impairment per abdominal pain, nausea, vomiting,
Mild to severe impairment: No dose weight loss) q2wks for 4 wks, then
adjustment. monthly thereafter (or as clinically indi-
Dosage in Hepatic Impairment
cated). Monitor for neurotoxicities. If
Mild impairment: No dose adjustment.
concomitant use of strong CYP3A inhibi-
Moderate to severe impairment: Re-
tor or strong CYP3A inducer is unavoid-
duce starting dose by 50%. able, monitor for drug toxicities. Dili-
gently screen for infections.
SIDE EFFECTS PATIENT/FAMILY TEACHING
Frequent (37%–15%): Fatigue, nausea, • Treatment may depress your immune
dizziness, cough, vomiting, constipation, system response and reduce your ability
diarrhea, pyrexia, dyspnea, increased to fight infection. Report symptoms of
weight, peripheral edema. Occasional infection such as body aches, chills,
(14%–11%): Arthralgia, myalgia, muscular cough, fatigue, fever. Avoid those with
weakness, headache, abdominal pain, active infection. • Nervous system
decreased appetite, back pain, extremity changes including altered memory, con-
pain, nasal congestion, hypertension. fusion, delirium, difficulty speaking, gait
ADVERSE EFFECTS/TOXIC disturbance, numbness, tremors may oc-
REACTIONS cur. Avoid tasks that require alertness,
motor skills if neurologic effects are oc-
Anemia, neutropenia is an expected re- curring. • Female pts and male pts with
sponse to therapy. Neurotoxic events in- female partners of childbearing potential
Canadian trade name Non-Crushable Drug High Alert drug
670 ledipasvir/sofosbuvir
must use effective contraception during without cirrhosis or with compensated
treatment and for at least 1 wk after last cirrhosis, in combination with ribavirin.
dose. Do not breastfeed. • Report liver
problems (abdominal pain, bruising, PRECAUTIONS
clay-colored stool, amber- or dark-col- Note: If used with ribavirin, the Contra-
ored urine, yellowing of the skin or indications and Cautions for the use of
eyes). • There is a high risk of interac- ribavirin also apply.
tions with other medications. Do not take Contraindications: Hypersensitivity to le-
newly prescribed medications unless ap- dipasvir, sofosbuvir. Cautions: Advanced
proved by prescriber who originally hepatic disease, HIV infection, hepatitis B
started treatment. • Avoid grapefruit virus infection. Concomitant use of amio-
products, herbal supplements (esp. St. darone (with or without beta blockers)
John’s wort). in pts with underlying cardiac disease.
Concomitant use of P-glycoprotein (P-
gp) inducers not recommended.

ledipasvir/sofosbuvir ACTION
Ledipasvir inhibits HCV NS5A protein, es-
le-dip-as-vir/soe-fos-bue-vir sential for viral replication. Sofosbuvir is
L (Harvoni) converted to its active form and inhibits
j BLACK BOX ALERT j Test NS5B RNA-dependent RNA polymerase,
all pts for hepatitis B virus (HBV) also essential for viral replication. Ther-
infection prior to initiation. HBV apeutic Effect: Inhibits viral replica-
reactivation was reported in HCV/
HBV co-infected pts who were tion of HCV.
undergoing or had completed treat-
ment with HCV direct-acting anti- PHARMACOKINETICS
virals and were not receiving HBV Widely absorbed. Ledipasvir is metabo-
antiviral therapy. HBV reactivation
may cause fulminant hepatitis, lized by oxidative processes. Sofosbuvir
hepatic failure, and death. is metabolized in liver. Protein binding:
Do not confuse ledipasvir with 99.8% (ledipasvir), 61%–65% (sofosbu-
daclatasvir, elbasvir, or ombitas- vir). Peak plasma concentration: 4–4.5
vir, or sofosbuvir with dasabuvir. hrs (ledipasvir), 0.8–1 hr (sofosbuvir).
Ledipasvir is excreted in feces (87%)
uCLASSIFICATION and urine (1%). Sofosbuvir is excreted in
PHARMACOTHERAPEUTIC: Combi- urine (80%), feces (14%). Half-life: 47
nation nucleotide analog NS5A in- hrs (ledipasvir), 0.4 hr (sofosbuvir).
hibitor and nucleotide analog NS5B
polymerase inhibitor. CLINICAL: An- LIFESPAN CONSIDERATIONS
tihepaciviral. Pregnancy/Lactation: Unknown if ledi-
pasvir or sofosbuvir is distributed in breast
milk. When administered with ribavirin,
USES therapy is contraindicated in pregnant
Treatment of chronic hepatitis C virus women and in men whose female partners
(HCV) in adults and children 12 yrs and are pregnant. Children: Safety and ef-
older or weighing at least 35 kg with ficacy not established in pts younger than
genotype 1, 4, 5, or 6 infection without 12 yrs of age or weight less than 35 kg. El-
cirrhosis or with compensated cirrhosis; derly: No age-related precautions noted.
genotype 1 infection in adults with de-
compensated cirrhosis, in combination INTERACTIONS
with ribavirin; genotype 1 or 4 infection in DRUG: May enhance bradycardic ef-
adults who are liver transplant recipients fect of amiodarone. May increase
underlined – top prescribed drug
ledipasvir/sofosbuvir 671
concentration of rosuvastatin. Alu- Genotype 1 or 4
minum- or magnesium-containing Treatment-naïve and treatment-
antacids, H2-receptor antagonists experienced liver transplant re-
(e.g., famotidine), proton pump cipients without cirrhosis or with
inhibitors (e.g., omeprazole), anti- compensated cirrhosis (Child-Pugh
convulsants (e.g., carBAMazepine), A): Ledipasvir/sofosbuvir plus ribavirin
antimycobacterials (e.g., rifAMPin) for 12 wks.
may decrease concentration/effects.
Treatment Regimen and Duration for
HERBAL: None significant. FOOD: None
Children
known. LAB VALUES: May increase serum
Genotype 1
bilirubin.
Treatment-naïve without cirrho-
AVAILABILITY (Rx) sis or with compensated cirrhosis
(Child-Pugh A): Ledipasvir/sofosbuvir
Tablets, Fixed-Dose Combination: 90 mg for 12 wks. Treatment-experienced
(ledipasvir)/400 mg (sofosbuvir). without cirrhosis: Ledipasvir/sofosbu-
ADMINISTRATION/HANDLING vir for 12 wks. Treatment-experienced
with compensated cirrhosis (Child-
PO Pugh A): Ledipasvir/sofosbuvir for
• Give without regard to food. 24 wks. L
Genotype 4, 5, or 6
INDICATIONS/ROUTES/DOSAGE Treatment-naïve and treatment-ex-
Hepatitis C Virus Infection perienced without cirrhosis or with
PO: ADULTS, ELDERLY, CHILDREN 12 YRS compensated cirrhosis (Child-Pugh
OF AGE AND OLDER, WEIGHING 35 KG OR A): Ledipasvir/sofosbuvir for 12 wks.
MORE: 1 tablet (ledipasvir/sofosbuvir)
once daily. See manufacturer guidelines Dosage in Renal Impairment
for treatment with ribavirin. Mild to moderate impairment: No
dose adjustment. Severe impairment:
Treatment Regimen and Duration for Not specified; use caution.
Adults
Genotype 1 Dosage in Hepatic Impairment
Treatment-naïve without cirrhosis or No dose adjustment.
with compensated cirrhosis (Child-
Pugh A): Ledipasvir/sofosbuvir for 12 SIDE EFFECTS
wks. Treatment for 8 wks may be con- Occasional (16%–4%): Fatigue, head-
sidered in treatment-naïve genotype 1 pts ache, nausea, diarrhea. Rare (3%): In-
without cirrhosis who have HCV-RNA level somnia. Ribavirin: Frequent (31%–29%):
less than 6 million international units/mL Asthenia, headache. Occasional (18%–
prior to initiation. Treatment-experi- 5%): Fatigue, myalgia, irritability, dizzi-
enced without cirrhosis: Ledipasvir/ ness. Rare (3%): Dyspnea.
sofosbuvir for 12 wks. Treatment-expe-
rienced with compe­nsated cirrhosis ADVERSE EFFECTS/TOXIC
(Child-Pugh A): Ledipasvir/sofosbuvir REACTIONS
for 24 wks. Ledipasvir/sofosbuvir plus HBV reactivation was reported in pts co-
ribavirin for 12 wks may be considered in infected with HBV/HCV; may result in ful-
treatment-experienced genotype 1 pts with minant hepatitis, hepatic failure, death.
cirrhosis who are eligible for ribavirin. Cardiac arrest, symptomatic bradycardia,
Treatment-naïve and treatment-ex- pacemaker implantation was reported
perienced with decompensated cir- in pts taking concomitant amiodarone.
rhosis (Child-Pugh B or C): Ledipasvir/ Bradycardia usually occurred within hrs
sofosbuvir plus ribavirin for 12 wks. to days, but may occur up to 2 wks after
Canadian trade name Non-Crushable Drug High Alert drug
672 leflunomide
initiation. Pts with underlying cardiac fainting, light-headedness, memory prob-
disease, advanced hepatic disease, or pts lems, palpitations, weakness. • Treat-
taking concomitant beta blockers are at ment may be used in combination with
an increased risk for bradycardia when ribavirin (inform pt of contraindications/
used concomitantly with amiodarone. adverse effects of ribavirin therapy). If
Psychiatric disorders including depres- therapy includes treatment with ribavirin,
sion may occur. females of reproductive potential and
males with female partners of reproductive
NURSING CONSIDERATIONS potential should avoid pregnancy during
treatment. • Do not breastfeed. • There
BASELINE ASSESSMENT
is an increased risk of drug interactions
Obtain LFT, HCV-RNA level; pregnancy with other medications. • Do not take
test in females of reproductive poten- newly prescribed medications unless ap-
tial; CBC for pts treated with ribavirin. proved by prescriber who originally started
Confirm HCV genotype. Test all pts for treatment. • Do not take herbal prod-
HBV infection prior to initiation. Re- ucts. • Avoid alcohol. • Report signs of
ceive full medication history and screen depression.
for contraindications/interactions, esp.
concomitant use of amiodarone. Ques-
L tion for history of chronic anemia, HBV
infection, HIV infection, liver transplan- leflunomide
tation.
lee-floo-noe-myde
INTERVENTION/EVALUATION
(Apo-Leflunomide , Arava)
Periodically monitor LFT, HCV-RNA level j BLACK BOX ALERT jDo not
for treatment effectiveness. Closely moni- use during pregnancy. Women
tor for exacerbation of hepatitis or HBV of childbearing potential must be
reactivation. If unable to discontinue counseled regarding fetal risk,
amiodarone, consider inpatient cardiac use of reliable contraceptives
confirmed, possibility of pregnancy
monitoring for at least 48 hrs, followed excluded. Severe hepatic injury
by outpatient or self-monitoring of heart may occur.
rate for at least 2 wks after initiation. Car-
diac monitoring is also recommended uCLASSIFICATION
in pts who discontinue amiodarone PHARMACOTHERAPEUTIC: Disease-
just prior to initiation. In females of modifying agent. CLINICAL: Anti-
reproductive potential who are taking rheumatic.
concomitant ribavirin, reinforce birth
control compliance and obtain monthly
pregnancy tests. Monitor for new-onset USES
or worsening of depression Treatment of active rheumatoid arthritis
(RA). Improve physical function in pts
PATIENT/FAMILY TEACHING with rheumatoid arthritis. OFF-LABEL:
• Pts who take amiodarone (an antiar- Treatment of cytomegalovirus (CMV) dis-
rhythmic) during therapy may require in- ease. Prevention of acute/chronic rejection
patient and outpatient cardiac monitoring in recipients of solid organ transplants.
(and in some cases pacemaker implanta-
tion) due to an increased risk of slow heart PRECAUTIONS
rate or cardiac arrest. If amiodarone ther- Contraindications:Hypersensitivity to
apy cannot be withheld or stopped, imme- lef­lunomide. Pregnancy or plans for
diately report symptoms of slow heart rate pregnancy. Severe hepatic impairment.
such as chest pain, confusion, dizziness, Concomitant use with teriflunomide.

underlined – top prescribed drug


leflunomide 673
Cautions: Hepatic/renal impairment, INDICATIONS/ROUTES/DOSAGE
hepatitis B or C virus infection, pts with Rheumatoid Arthritis (RA)
immunodeficiency or bone marrow dys- PO: ADULTS, ELDERLY: Initially, 100 mg/
plasias, breastfeeding mothers, history day for 3 days, then 10–20 mg/day. (Load-
of new/recurrent infections, latent TB, ing dose may be omitted in pts at increased
significant hematologic abnormalities, risk of hepatic or hematologic toxicity.)
diabetes, concomitant use of neurotoxic
medications, elderly pts. Dosage in Renal Impairment
No dose adjustment.
ACTION
Inhibits pyrimidine synthesis, resulting in Dosage in Hepatic Impairment
antiproliferative and anti-inflammatory ef- ALT 2–3 times upper limit of normal
fects. Therapeutic Effect: Reduces signs/ (ULN): Not recommended. Persis-
symptoms of RA, retards structural damage. tent ALT level greater than 3 times
ULN: Discontinue and initiate acceler-
PHARMACOKINETICS ated drug elimination. Cholestyramine
Well absorbed after PO administration. 8 g 3 times/day for 11 days or activated
Protein binding: greater than 99%. Metab- charcoal 50 g q12h for 11 days.
olized in GI wall, liver. Excreted through
renal, biliary systems. Not removed by he- SIDE EFFECTS L
modialysis. Half-life: 16 days. Frequent (20%–10%): Diarrhea, respira-
tory tract infection, alopecia, rash, nausea.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Can cause ADVERSE EFFECTS/TOXIC
fetal harm. Contraindicated in preg- REACTIONS
nancy. Unknown if distributed in breast May cause immunosuppression. Tran-
milk. Breastfeeding not recommended. sient thrombocytopenia, leukopenia,
Children: Safety and efficacy not es- hepatotoxicity occur rarely. Interstitial
tablished. Elderly: No age-related pre- lung disease, peripheral neuropathy.
cautions noted.
NURSING CONSIDERATIONS
INTERACTIONS BASELINE ASSESSMENT
DRUG: RifAMPin may increase concen- Obtain pregnancy test in females of repro-
tration/effects. Hepatotoxic medications ductive potential. Question plans of breast-
(e.g., acetaminophen, ketoconazole, feeding. Obtain baseline CBC, LFT. Assess
simvastatin) may increase risk of side limitations in activities of daily living due to
effects, hepatotoxicity. May decrease the rheumatoid arthritis (RA). Obtain baseline
therapeutic effect of BCG (intravesi- evaluation for active TB, latent TB.
cal), nivolumab, vaccines (live). May
increase adverse effects of natalizumab, INTERVENTION/EVALUATION
vaccines (live). HERBAL: Echinacea Monitor tolerance to medication. Assess
may decrease effects. FOOD: None known. symptomatic relief of RA (relief of pain;
LAB VALUES: May increase serum ALT, improved range of motion, grip strength,
AST, alkaline phosphatase, bilirubin. mobility). Monitor LFT, CBC, signs/symp-
toms of severe infection or pulmonary
AVAILABILITY (Rx) symptoms.
Tablets: 10 mg, 20 mg.
PATIENT/FAMILY TEACHING
ADMINISTRATION/HANDLING • May take without regard to food.
PO • Improvement may take longer than 8
• Give without regard to food. wks. • Avoid pregnancy.

Canadian trade name Non-Crushable Drug High Alert drug


674 lenalidomide

ACTION
lenalidomide Inhibits secretion of pro-inflammatory
cytokines, increases secretion of anti-
len-a-lid-o-myde
inflammatory cytokines. Enhances cell-
(Revlimid)
mediated immunity by stimulation of
j BLACK BOX ALERT jAnalogue T cells. Therapeutic Effect: Inhibits
to thalidomide. High potential for
significant birth defects. Hemato- myeloma cell growth; induces cell cycle
logic toxicity (thrombocytopenia, arrest and cell death.
neutropenia) occurs in 80% of pts.
Greatly increases risk for DVT, PHARMACOKINETICS
pulmonary embolism in multiple Well absorbed following PO administra-
myeloma pts.
Do not confuse lenalidomide tion. Protein binding: 30%. Excreted in
with thalidomide. urine. Half-life: 3 hrs (increased in
renal impairment).
uCLASSIFICATION
LIFESPAN CONSIDERATIONS
PHARMACOTHERAPEUTIC: Angio-
genesis inhibitor. CLINICAL: Anti- Pregnancy/Lactation: Contraindi-
neoplastic. cated in women who are or may become
pregnant, who are not using two reliable
L forms of contraception, or who are not
USES abstinent. Can cause severe birth defects,
fetal death. Unknown if distributed in
Treatment of low- to intermediate-risk my- breast milk; breastfeeding not recom-
elodysplastic syndrome (MDS) in pts with mended. Children: Safety and efficacy
deletion 5q cytogenetic abnormality with not established. Elderly: Age-related
transfusion-dependent anemia. Treatment renal impairment may require caution in
of multiple myeloma (in combination with dosage selection. Risk of toxic reactions
dexamethasone). Treatment of pts with greater in those with renal insufficiency.
mantle cell lymphoma that has relapsed or
progressed after 2 prior therapies (one of INTERACTIONS
which included bortezomib). Maintenance DRUG: May increase toxic effects of
treatment for multiple myeloma (fol- abatacept, anakinra, bisphospho-
lowing autologous stem cell transplant). nate derivatives, canakinumab, leflu-
Treatment of previously treated follicular nomide, natalizumab, nivolumab,
lymphoma (in combination with rITUX- rilonacept, tofacitinib, vedolizumab.
imab). Treatment of previously treated May increase immunosuppressive ef-
marginal zone lymphoma (in combination fects of certolizumab, fingolimod,
with riTUXimab). OFF-LABEL: Systemic ocrelizumab. Denosumab, dipy-
amyloidosis, lower-risk myelodysplastic rone, pimecrolimus may increase risk
syndrome, non-Hodgkin’s lymphoma. Re- of toxicity. May decrease therapeutic ef-
lapsed or refractory chronic lymphocytic fect of nivolumab. Dexamethasone,
leukemia (CLL). erythropoiesis-stimulating agents,
PRECAUTIONS estrogens may increase risk of thrombo-
sis. Ocrelizumab, roflumilast, tocili-
Contraindications: Hypersensitivity to le- zumab may increase immunosuppressive
nalidomide. Pregnancy, women capable effects. May increase concentration effect
of becoming pregnant. Cautions: Renal/ of digoxin. May increase adverse effects/
hepatic impairment. History of arterial decrease therapeutic of vaccines (live).
thromboembolic events, hypertension, HERBAL: Echinacea may decrease ther-
hyperlipidemia. Avoid use in pts with glu- apeutic effect. FOOD: None known. LAB
cose intolerance, lactase deficiency. VALUES: May decrease WBC count, Hgb,

underlined – top prescribed drug


lenalidomide 675
Hct platelets, troponin I, serum creatinine, neutrophil count (ANC) 1,000/mcl
sodium, T3, T4. May decrease serum bili- or greater: If ANC less than 750 cells/
rubin, glucose, potassium, magnesium. mm3, hold treatment. Resume at 5 mg/
day when ANC 1,000 cells/mm3 or greater.
AVAILABILITY (Rx) Baseline ANC less than 1,000 cells/
Capsules: 2.5 mg, 5 mg, 10 mg, 15 mm3: If ANC less than 500 cells/mm3,
mg, 20 mg, 25 mg. hold treatment. Resume at 5 mg/day when
ANC 500 cells/mm3 or greater.
ADMINISTRATION/HANDLING Neutropenia after 4 wks with 10 mg/
• Store at room temperature. • Do not day: If ANC less than 500 cells/mm3 for
break, crush, dissolve, or divide cap- 7 days or longer or associated with fever,
sules. • Swallow whole with water. hold treatment. Resume at 5 mg/day when
ANC 500 cells/mm3 or greater.
INDICATIONS/ROUTES/DOSAGE Neutropenia developing with 5 mg/
Myelodysplastic Syndrome day: If ANC less than 500 cells/mm3 for 7
PO: ADULTS, ELDERLY: 10 mg once daily. days or longer or associated with fever, hold
Continue until disease progression or un- treatment. Resume at 5 mg every other day
acceptable toxicity. when ANC 500 cells/mm3 or greater.

Dosage Adjustments for Myelodysplastic Follicular Lymphoma, Marginal Zone L


Syndrome Lymphoma
Platelets PO: ADULTS, ELDERLY: 20 mg once daily
Thrombocytopenia within 4 wks for 21 days of 28-day cycle (in combina-
with 10 mg/day: Baseline platelets tion with riTUXimab) for up to 12 cycles.
100,000 cells/mm3 or greater: If
Mantle Cell Lymphoma
platelets less than 50,000 cells/mm3, hold
treatment. Resume at 5 mg/day when plate- PO: ADULTS, ELDERLY: 25 mg once daily
lets return to 50,000 cells/mm3 or greater. on days 1–21 of repeated 28-day cycle.
Baseline platelets less than 100,000 Continue until disease progression or un-
cells/mm3: If platelets fall to 50% of base- acceptable toxicity.
line, hold treatment. Resume at 5 mg/day Multiple Myeloma
if baseline is 60,000 cells/mm3 or greater PO: ADULTS, ELDERLY: 25 mg/day on days
and platelets return to 50,000 cells/mm3 1–21 of repeated 28-day cycle (in com-
or greater. Resume at 5 mg/day if baseline bination with dexamethasone). Continue
is less than 60,000 cells/mm3 and platelets until disease progression or unacceptable
return to 30,000 cells/mm3 or greater. toxicity. If eligible for transplant, HSCT mo-
Thrombocytopenia after 4 wks with bilization should occur within 4 cycles of
10 mg/day: If platelets less than 30,000 lenalidomide-containing therapy.
cells/mm3 OR less than 50,000 cells/mm3
with platelet transfusion, hold treatment. Multiple Myeloma Following Auto-HSCT
Resume at 5 mg/day when platelets re- PO: ADULTS, ELDERLY: 10 mg once daily
turn to 30,000 cells/mm3 or greater. continuously on days 1–28 of repeated
Thrombocytopenia developing with 28-day cycle. If tolerated, may increase
5 mg/day: If platelets less than 30,000 to 15 mg once daily after 3 cycles.
cells/mm3 OR less than 50,000 cells/mm3
with platelet transfusion, hold treatment. Dosage Adjustments for Multiple Myeloma
Resume at 5 mg every other day when plate- Thrombocytopenia: If platelets fall to
lets return to 30,000 cells/mm3 or greater. less than 30,000 cells/mm3, hold treat-
Neutrophils ment, monitor CBC. Resume at 15 mg/
Neutropenia within 4 wks with day when platelets 30,000 cells/mm3 or
10 mg/day: Baseline absolute greater. For each subsequent fall to less
Canadian trade name Non-Crushable Drug High Alert drug
676 lenalidomide
than 30,000 cells/mm3, hold treatment 1,000 cells/mm3 and neutropenia is the
and resume at 5 mg/day less than previ- only toxicity. Resume at 15 mg/day if
ous dose when platelets return to 30,000 other toxicity is present. For each subse-
cells/mm3 or greater. Do not dose to less quent fall to less than 1,000 cells/mm3,
than 5 mg/day. hold treatment and resume at 5 mg/day
Neutropenia: If neutrophils fall to less less than previous dose when neutrophils
than 1,000 cells/mm3, hold treatment, return to 1,000 cells/mm3 or greater. Do
add G-CSF, follow CBC wkly. Resume at not dose to less than 5 mg/day.
25 mg/day when neutrophils return to

Creatinine Creatinine Clearance Creatinine Clearance


Dosage in Renal Clearance Less Than 30 mL/min Less Than 30 mL/min
Impairment 30–59 mL/min (Non-dialysis Dependent) (Dialysis Dependent)
Myelodysplastic 5 mg once 2.5 mg once daily 2.5 mg once daily
syndrome daily (give after dialysis)
Multiple myeloma 10 mg once 15 mg q48h 5 mg once daily (give
daily after dialysis)
L

Dosage in Hepatic Impairment


NURSING CONSIDERATIONS
No dose adjustment.
BASELINE ASSESSMENT
SIDE EFFECTS Obtain baseline CBC. Due to high potential
Frequent (49%–31%): Diarrhea, pru- for human birth defects/fetal death, female
ritus, rash, fatigue. Occasional (24%– pts must avoid pregnancy 4 wks before
12%): Constipation, nausea, arthralgia, therapy, during therapy, during dose in-
fever, back pain, peripheral edema, terruptions, and 4 wks following therapy.
cough, dizziness, headache, muscle Two reliable forms of contraception must
cramps, epistaxis, asthenia, dry skin, ab- be used even if pt has history of infertil-
dominal pain. Rare (10%–5%): Extremity ity unless it is due to hysterectomy or
pain, vomiting, generalized edema, an- menopause that has occurred for at least
orexia, insomnia, night sweats, myalgia, 24 consecutive mos. Confirm two nega-
dry mouth, ecchymosis, rigors, depres- tive pregnancy tests before therapy ini-
sion, dysgeusia, palpitations. tiation. Screen for risk of arterial, venous
thrombosis. Offer emotional ­support.
ADVERSE EFFECTS/TOXIC
REACTIONS INTERVENTION/EVALUATION
Significant increased risk of deep Monitor CBC, BMP, serum magnesium
vein thrombosis (DVT), pulmonary as appropriate. Perform pregnancy tests
embolism. Thrombocytopenia occurs on women of childbearing potential:
in 62% of pts, neutropenia in 59% of wkly during the first 4 wks, then at 4-wk
pts, and anemia in 12% of pts. Upper ­intervals in pts with regular menstrual
respiratory infection (nasopharyngitis, cycles or q2wks in pts with irregular
pneumonia, sinusitis, bronchitis, rhini- menstrual cycles. Monitor for hemato-
tis), UTI occur occasionally. Cellulitis, logic toxicity; obtain CBC wkly during
peripheral neuropathy, hypertension, first 8 wks of therapy and at least monthly
hypothyroidism occur in approximately thereafter. Observe for signs, symptoms
6% of pts. of thromboembolism (shortness of
underlined – top prescribed drug
lenvatinib 677
breath, chest pain, extremity pain, swell- renal impairment. History of cardiac dys-
ing, stroke-like symptoms). function (HF, pulmonary edema, right or
left ventricular dysfunction), GI perforation/
PATIENT/FAMILY TEACHING
hemorrhage, hypertension, long QT interval
• Two reliable forms of birth control syndrome, medications that prolong QT
must be used at least 4 wks before, dur- interval, thromboembolic events (e.g., CVA,
ing, and for 4 wks following therapy. • A DVT), pituitary/thyroid disease.
pregnancy test must be performed within
10–14 days and 24 hrs before therapy ACTION
begins. • Males must always use a latex Inhibits tyrosine kinase receptor activ-
or synthetic condom during any sexual ity of vascular endothelial growth factor
contact with females of childbearing po- (VEGF) receptors. Inhibits tumor angio-
tential even if they have undergone a suc- genesis, growth, progression. Thera-
cessful vasectomy. • Avoid crowds; avoid peutic Effect: Decreases tumor cell
those with active infection. • Treatment growth, slows cancer progression.
may cause blood clots in the arms, legs, or
lungs; report arm or leg pain/swelling, PHARMACOKINETICS
difficulty breathing, chest pain. Readily absorbed. Metabolized in liver.
Protein binding: 98%–99%. Peak plasma
concentration: 1–4 hrs. Excreted in feces L
(64%), urine (25%). Not removed by di-
lenvatinib alysis. Half-life: 28 hrs.
len-va-ti-nib LIFESPAN CONSIDERATIONS
(Lenvima) Pregnancy/Lactation: Avoid pregnan­cy;
Do not confuse lenvatinib with may cause fetal harm. Female pts of repro-
dasatinib, ibrutinib, imatinib. ductive potential must use effective contra-
ception during treatment for at least 2 wks
uCLASSIFICATION
after discontinuation. Potentially distributed
PHARMACOTHERAPEUTIC: Vascular in breast milk. Must either discontinue drug
endothelial growth factor (VEGF) or discontinue breastfeeding. Treatment
inhibitor. Tyrosine kinase inhibitor. may reduce fertility in both female and male
CLINICAL: Antineoplastic. pts. Children: Safety and efficacy not es-
tablished. Elderly: No age-related precau-
tions noted.
USES
Treatment of locally recurrent or metastatic, INTERACTIONS
progressive, radioactive iodine–refractory DRUG: CYP3A4 inhibitors (e.g., ke-
differentiated thyroid cancer. Treatment toconazole, ritonavir) may increase
of advanced renal cell carcinoma (RCC) concentration/effect. May increase
in combination with everolimus after one QT-prolonging effect of amiodarone,
course of another antineoplastic. First-line citalopram, clarithromycin, moxi-
treatment of unresectable hepatocellular floxacin, nilotinib, quetiapine, ri-
carcinoma (HCC). Treatment of advanced bociclib, thioridazine. HERBAL: None
endometrial carcinoma (in combination significant. FOOD: None known. LAB
with pembrolizumab). VALUES: May increase serum alkaline
phosphatase, ALT/AST, amylase, bilirubin,
PRECAUTIONS cholesterol, creatinine, lipase. May de-
Contraindications: Hypersensitivity to len­ crease serum albumin, glucose, magne-
vatinib. Cautions: Electrolyte imbalance sium; platelets. May increase or decrease
(hypokalemia, hypomagnesemia), hepatic/ serum calcium, potassium.

Canadian trade name Non-Crushable Drug High Alert drug


678 lenvatinib

AVAILABILITY (Rx) Adjusted


Dose
Capsules: 4 mg, 10 mg.
Adverse (Thyroid
ADMINISTRATION/HANDLING Reaction Modification Cancer)
PO Second Interrupt until 14 mg
­occurrence resolved to once
• Give without regard to food. • Ad- Grade 0 or 1 or daily
minister same time each day. • Do not baseline
cut, crush, divide, or open cap- Third Interrupt until 10 mg
sules. • Should be swallowed whole. ­occurrence resolved to once
May be dissolved with 15 mL water or Grade 0 or 1 or daily
apple juice by first adding whole capsule baseline
to liquid; leave for 10 min, stir for 3 min,
then administer. Then add 15 mL to Adjusted dose for RCC is lower. 14 mg for
glass, swirl, swallow additional liquid. first occurrence, 10 mg for second oc-
currence, 8 mg for third occurrence.
INDICATIONS/ROUTES/DOSAGE
Thyroid Cancer Arterial Thrombotic Event
PO: ADULTS, ELDERLY: 24 mg once daily. Discontinue treatment.
L Continue until disease progression or un- Cardiac Dysfunction/Hemorrhagic Event
acceptable toxicity. PO: ADULTS, ELDERLY: Interrupt treatment
for Grade 3 event until improved to Grade
RCC
0 to 1 or baseline. Either resume at re-
PO: ADULTS, ELDERLY: 18 mg once daily
duced dose or discontinue (depending
(in combination with everolimus). Con-
on the severity and persistence). Discon-
tinue until disease progression or unac-
tinue for Grade 4 event.
ceptable toxicity.
GI Perforation/Fistula Formation
HCC
Discontinue treatment.
PO: ADULTS, ELDERLY: (60 KG OR
GREATER): 12 mg once daily. (LESS THAN 60 Hypertension
KG): 8 mg once daily. Continue until dis- PO: ADULTS, ELDERLY: Interrupt treat-
ease progression or unacceptable toxicity. ment for Grade 3 hypertension that
persists despite optimal antihypertensive
Endometrial Carcinoma (Advanced) therapy. Resume at reduced dose when
PO: ADULTS, ELDERLY: 20 mg once daily hypertension is controlled at less than
(in combination with pembrolizumab). or equal to Grade 2. Discontinue for life-
Continue until disease progression or threatening hypertension.
unacceptable toxicity.
Proteinuria
Dose Modification PO: ADULTS, ELDERLY: Interrupt treat-
Based on Common Terminology Criteria ment for greater than or equal to 2 g
for Adverse Events (CTCAE). proteinuria/24 hrs. Resume at reduced
Adjusted dose when proteinuria less than 2 g/24
Dose hrs. Discontinue if nephrotic syndrome
Adverse (Thyroid occurs.
Reaction Modification Cancer)
First Interrupt until 20 mg QT Prolongation
­occurrence resolved to once PO: ADULTS, ELDERLY: Interrupt treat-
Grade 0 or 1 or daily ment for Grade 3 or greater. Resume at
baseline reduced dose when QT prolongation re-
solved to Grade 0 or 1 or baseline.

underlined – top prescribed drug


lenvatinib 679
Renal Failure/Impairment or of pts); hepatotoxicity (4% of pts); hyper-
Hepatotoxicity tension (73% of pts); Grade 3 or greater
PO: ADULTS, ELDERLY: Interrupt treatment hypocalcemia (9% of pts); impairment of
for Grade 3 or 4 renal failure/impairment thyroid-stimulating hormone (57% of pts);
or hepatotoxicity until resolved to Grade 0 palmar-plantar erythrodysesthesia (32% of
or 1 or baseline. Either resume at reduced pts); proteinuria (34% of pts); QT inter-
dose or discontinue (depending on the val prolongation (9% of pts); renal failure
severity and persistence). Discontinue if (14% of pts); urinary tract infection (11%
hepatic failure occurs. of pts). Reverse posterior leukoencepha-
lopathy occurs rarely. The median onset
Reversible Posterior of hypertension was 16 days. The most
Leukoencephalopathy Syndrome (RPLS) frequently reported hemorrhagic event was
PO: ADULTS, ELDERLY: Interrupt treatment epistaxis. The primary risk factor for renal
until fully resolved. Resume at reduced dose failure was dehydration and hypovolemia
or discontinue (depending on the severity related to diarrhea and vomiting.
and persistence of neurologic symptoms).
Other Adverse Reactions NURSING CONSIDERATIONS
PO: ADULTS, ELDERLY: Reduce dose ac- BASELINE ASSESSMENT
cording to dose modification table. Due Obtain baseline CBC, BMP, LFT; serum L
to limited data, there are no recommen- magnesium, phosphate, ionized calcium;
dations on resuming treatment in pts urinalysis for proteinuria. Confirm negative
with Grade 4 adverse events that resolve. pregnancy status before initiating treat-
Dosage in Renal/Hepatic Impairment ment. Receive full medication history and
Mild to moderate impairment: No screen for interactions. Question history of
dose adjustment. Severe impairment: cardiac/pituitary/thyroid disease, CVA/DVT,
14 mg once daily. hypertension, hepatic/renal impairment,
long QT interval syndrome. Assess oral cav-
SIDE EFFECTS ity for lesions, poor dentation. Ensure that
Frequent (73%–29%): Hypertension, diar- B/P is controlled prior to initiation. Assess
rhea, fatigue, asthenia, malaise, arthralgia, hydration status. Offer emotional support.
myalgia, decreased appetite, weight de- INTERVENTION/EVALUATION
creased, nausea, stomatitis, glossitis, mouth Monitor B/P after 1 wk, then every 2 wks for
ulceration, mucosal inflammation, head- the first 2 mos, then at least monthly there-
ache, vomiting, dysphonia, abdominal pain, after. Monitor LFT every 2 wks for the first 2
constipation. Occasional (25%–7%): Oral mos, then at least monthly thereafter. Moni-
pain, glossodynia, cough, peripheral tor for proteinuria periodically. If urine dip-
edema, rash, dysgeusia, dry mouth, dizzi- stick proteinuria is greater than or equal to
ness, dyspepsia, insomnia, alopecia, hypo- 2+, obtain a 24-hr urine protein test. Moni-
tension, dehydration, hyper­keratosis. tor blood calcium levels at least monthly
ADVERSE EFFECTS/TOXIC and replace as needed depending on sever-
REACTIONS ity, presence of ECG changes, persistence
of hypocalcemia. Monitor and correct
Serious adverse effects may include arte- other electrolyte abnormalities as needed.
rial thromboembolic events (5% of pts); Initiate medical management for nausea,
cardiac dysfunction (7% of pts); dental vomiting, diarrhea prior to any interrup-
and oral infections including gingivitis, tion or dose reduction. Reversible posterior
parotitis, pericoronitis, periodontitis, si- leukoencephalopathy syndrome should be
aloadenitis, tooth abscess, tooth infection considered in pts with altered mental status,
(10% of pts); GI perforation/fistula forma- confusion, headache, seizures, visual dis-
tion (2% of pts); hemorrhagic events (35%
Canadian trade name Non-Crushable Drug High Alert drug
680 letrozole
turbances. Immediately report abdominal USES
pain, GI bleeding, hemoptysis (may indicate First-line treatment of hormone recep-
GI perforation/fistula formation). Obtain tor–positive or hormone receptor un-
cardiac echocardiogram, ECG if cardiac known locally advanced or metastatic
decompensation is suspected. breast cancer. Treatment of advanced
PATIENT/FAMILY TEACHING breast cancer in postmenopausal women
• Blood levels will be monitored regu- with disease progression following anti-
larly. • Treatment may cause fetal harm. estrogen therapy. Postsurgical treatment
Female pts of childbearing potential for postmenopausal women with hor-
should use effective contraception during mone receptor–positive early breast can-
treatment and up to 2 wks following cer. Extended treatment of early breast
­discontinuation. Immediately report sus- cancer after 5 yrs of tamoxifen. OFF-
pected pregnancy. • Therapy may re- LABEL: Treatment of ovarian (epithelial),
duce fertility in both female and male endometrial cancer.
pts. • Report liver problems such as up- PRECAUTIONS
per abdominal pain, bruising, dark or
amber-colored urine, nausea, vomiting, or Hypersensitivity to letro­
Contraindications:
yellowing of the skin or eyes; heart prob- zole, other aromatase inhibitors. Use in
lems such as chest tightness, dizziness, women who are or may become preg-
L
fainting, palpitations, shortness of breath; nant. Cautions: Hepatic impairment, hy-
kidney problems such as dark-colored perlipidemia.
urine, decreased urine output, extremity ACTION
swelling, flank pain; skin changes such as
rash, skin bubbling, sloughing. • Neuro- Decreases circulating estrogen by inhibit-
logic changes including blurry vision, con- ing aromatase, an enzyme that catalyzes
fusion, headache, one-sided weakness, the final step in estrogen production
seizures, trouble speaking may indicate (inhibits conversion of androgens to es-
high blood pressure crisis, stroke, or life- trogens). Therapeutic Effect: Inhibits
threatening brain swelling. • Report growth of breast cancers stimulated by
mouth ulceration, jaw pain. • Swallow estrogens.
capsules whole; do not chew, crush, cut, PHARMACOKINETICS
or open capsules. • Treatment may in-
crease risk of GI bleeding, nose- Rapidly, completely absorbed. Metabo-
bleeds. • Drink plenty of fluids. lized in liver. Primarily excreted in urine.
Unknown if removed by hemodialysis.
Half-life: Approximately 2 days.
LIFESPAN CONSIDERATIONS
letrozole Pregnancy/Lactation: Unknown if
distributed in breast milk. May cause fe-
let-roe-zole tal harm. Children: Safety and efficacy
(Femara) not established. Elderly: No age-related
Do not confuse Femara with precautions noted.
Famvir, Femhrt, or Provera, or
letrozole with anastrozole. INTERACTIONS
DRUG: Tamoxifen may reduce con-
uCLASSIFICATION centration. HERBAL: None significant.
PHARMACOTHERAPEUTIC: Aro- FOOD: None known. LAB VALUES: May
matase inhibitor, hormone. CLINICAL: increase serum calcium, cholesterol,
Antineoplastic. GGT, ALT, AST, bilirubin.

underlined – top prescribed drug


leucovorin 681

AVAILABILITY (Rx) to beginning therapy. Offer emotional


Tablets: 2.5 mg. support.
INTERVENTION/EVALUATION
ADMINISTRATION/HANDLING
Assist with ambulation if asthenia, dizzi-
PO ness occurs. Assess for headache. Offer
• Give without regard to food. antiemetic for nausea, vomiting. Monitor
INDICATIONS/ROUTES/DOSAGE CBC, thyroid function, electrolytes, renal
function, LFT. Monitor for evidence of
Breast Cancer (Advanced) musculoskeletal pain; offer analgesics
PO: ADULTS, ELDERLY: 2.5 mg/day. Con- for pain relief.
tinue until tumor progression is evident.
PATIENT/FAMILY TEACHING
Breast Cancer (Early–Adjuvant Treatment) • Report if nausea, asthenia, hot flashes
PO: ADULTS, ELDERLY: (Postmenopausal): become unmanageable. • Discuss im-
2.5 mg/day for planned duration of 5 yrs. portance of negative pregnancy test prior to
Discontinue at relapse. beginning therapy; discuss nonhormonal
Breast Cancer (Early–Extended Adjuvant
methods of birth control. • Explain pos-
Treatment)
sible risk to fetus if pt is or becomes preg-
PO: ADULTS, ELDERLY: (Postmenopausal):
nant before or during therapy. L
2.5 mg/day for planned duration of 5 yrs
(after 5 yrs of tamoxifen). Discontinue at
relapse. leucovorin
Dosage in Renal Impairment loo-koe-vor-in
No dose adjustment. Do not confuse leucovorin with
Dosage in Severe Hepatic Impairment
Leukeran.
PO: ADULTS, ELDERLY: 2.5 mg every uCLASSIFICATION
other day.
PHARMACOTHERAPEUTIC: Rescue
SIDE EFFECTS agent (chemotherapy). CLINICAL:
Frequent (21%–9%): Musculoskeletal pain Antidote.
(back, arm, leg), nausea, headache.
Occasional (8%–5%): Constipation, ar- USES
thralgia, fatigue, vomiting, hot flashes,
Treatment of megaloblastic anemias
diarrhea, abdominal pain, cough, rash,
when folate deficient. Palliative treatment
anorexia, hypertension, peripheral
of advanced colon cancer (with fluoro-
edema. Rare (4%–1%): Asthenia, drowsi-
uracil). IV rescue therapy after high-dose
ness, dyspepsia, weight gain, pruritus.
methotrexate for osteosarcoma or orally
ADVERSE EFFECTS/TOXIC to diminish toxicity and impaired metho-
REACTIONS trexate elimination. OFF-LABEL: Adjunc-
tive cofactor therapy in methanol toxicity.
Pleural effusion, pulmonary embolism,
Prevents pyrimethamine hematologic tox-
bone fracture, thromboembolic disorder,
icity in HIV-positive pts.
MI occur rarely.
PRECAUTIONS
NURSING CONSIDERATIONS
Contraindications: Hypersensitivity to leu­
BASELINE ASSESSMENT co­vorin. Pernicious anemia, other mega-
Obtain baseline CBC, chemistries, renal loblastic anemias secondary to vitamin B12
function, LFT. Obtain pregnancy test prior deficiency. Cautions: Renal impairment.

Canadian trade name Non-Crushable Drug High Alert drug


682 leucovorin

ACTION Reconstitution • Reconstitute each 50-


Actively competes with methotrexate for mg vial with 5 mL Sterile Water for Injec-
same transport processes into cells, dis- tion or Bacteriostatic Water for Injection
places methotrexate from intracellular containing benzyl alcohol to provide con-
binding sites, and restores active folate centration of 10 mg/mL. • Due to benzyl
stores necessary for DNA/RNA synthe- alcohol in 1-mg ampule and in Bacterio-
sis. Therapeutic Effect: Reverses toxic static Water for Injection, reconstitute
effects of folic acid antagonists. Reverses doses greater than 10 mg/m2 with Sterile
folic acid deficiency. Water for Injection. • Further dilute with
100–1,000 mL D5W or 0.9% NaCl.
PHARMACOKINETICS Rate of administration • Do not ex-
Readily absorbed from GI tract. Widely ceed 160 mg/min if given by IV infusion
distributed. Metabolized in liver, in- (due to calcium content).
testinal mucosa. Primarily excreted in Storage • Store powdered vials for
urine. Half-life: 15 min; metabolite, parenteral use at room tempera-
30–35 min. ture. • Refrigerate solution for injec-
tion vials. • Injection appears as clear,
LIFESPAN CONSIDERATIONS yellowish solution. • Use immediately if
Pregnancy/Lactation: Unknown if reconstituted with Sterile Water for Injec-
L drug crosses placenta or is distributed tion; stable for 7 days if reconstituted
in breast milk. Children: May increase with Bacteriostatic Water for Injection.
risk of seizures by counteracting anti- Diluted solutions stable for 24 hrs at
convulsant effects of barbiturates, hy- room temperature or 4 days refrigerated.
dantoins. Elderly: Age-related renal PO
impairment may require dosage adjust- • Scored tablets may be crushed.
ment when used for rescue from effects
of high-dose methotrexate therapy. IV INCOMPATIBILITIES
Amphotericin B complex (Abelcet, Am-
INTERACTIONS Bisome, Amphotec), droperidol (Inap-
DRUG: May decrease effects of trim- sine), foscarnet (Foscavir).
ethoprim, anticonvulsants (e.g.,
phenytoin). May increase 5-fluoro- IV COMPATIBILITIES
uracil toxicity/effects when taken in CISplatin (Platinol AQ), cyclophospha-
combination. HERBAL: None significant. mide (Cytoxan), DOXOrubicin (Adria-
FOOD: None known. LAB VALUES: May mycin), etoposide (VePesid), filgrastim
decrease platelets, WBCs (when used in (Neupogen), 5-fluorouracil, gemcitabine
combination with 5-fluorouracil). (Gemzar), granisetron (Kytril), heparin,
methotrexate, metoclopramide (Reglan),
AVAILABILITY (Rx) mitoMYcin (Mutamycin), piperacillin
50
Injection, Powder for Reconstitution: and tazobactam (Zosyn), vinBLAStine
mg, 100 mg, 200 mg, 350 mg, 500 mg. (Velban), vinCRIStine (Oncovin).
Injection, Solution: 10 mg/mL. Tablets:
5 mg, 10 mg, 15 mg, 25 mg. INDICATIONS/ROUTES/DOSAGE
Rescue in High-Dose Methotrexate
ADMINISTRATION/HANDLING Therapy
IV PO, IV, IM: ADULTS, ELDERLY, CHIL-
DREN: 15 mg (approximately 10 mg/m2)
b ALERT c Strict adherence to timing started 24 hrs after starting methotrex-
of 5-fluorouracil following leucovorin ate infusion; continue q6h for 10 doses,
therapy must be maintained. until methotrexate level is less than 0.05

underlined – top prescribed drug


leuprolide 683
micromole/L. Additional dose adjusted Observe elderly, debilitated closely due
based on methotrexate levels. to risk for severe toxicities. Assess CBC,
BMP, LFT.
Folic Acid Antagonist Overdose
PO: ADULTS, ELDERLY, CHILDREN: 5–15 PATIENT/FAMILY TEACHING
mg/day. • Explain purpose of medication in
treatment of cancer. • Report allergic
Megaloblastic Anemia Secondary to
reaction, vomiting.
Folate Deficiency
IM/IV: ADULTS, ELDERLY, CHILDREN: 1
mg or less per day.
Colon Cancer leuprolide
b ALERT c For rescue therapy in can-
cer chemotherapy, refer to specific pro- loo-proe-lide
tocols used for optimal dosage and se- (Eligard, Lupron , Lupron Depot,
quence of leucovorin administration. Lupron Depot-Ped)
IV: ADULTS, ELDERLY: (In Combination
uCLASSIFICATION
with 5-fluorouracil): 200 mg/m2 daily
for 5 days. Repeat course at 4-wk inter- PHARMACOTHERAPEUTIC: Gonad-
vals for 2 courses, then 4- to 5-wk inter- otropin-releasing hormone (GnRH) L
vals or 20 mg/m2 daily for 5 days. Repeat analogue. CLINICAL: Antineoplastic.
course at 4-wk intervals for 2 courses,
then 4- to 5-wk intervals.
USES
Dosage in Renal/Hepatic Impairment Palliative treatment of advanced prostate
No dose adjustment. carcinoma. Management of endometrio-
sis. Treatment of anemia caused by uterine
SIDE EFFECTS leiomyomata (fibroids). Treatment of cen-
Frequent: When combined with chemo- tral precocious puberty. OFF-LABEL: Treat-
therapeutic agents: diarrhea, stomatitis, ment of breast cancer, infertility.
nausea, vomiting, lethargy, malaise, fatigue,
alopecia, anorexia. Occasional: Urticaria, PRECAUTIONS
dermatitis. Contraindications: Hypersensitivity to le-
uprolide, GnRH, GnRH-agonist analogue.
ADVERSE EFFECTS/TOXIC Pregnancy or women who may become
REACTIONS pregnant, breastfeeding (Lupron De-
Excessive dosage may negate chemother- pot 3.75 mg and 11.25 mg), abnormal,
apeutic effects of folic acid antagonists. undiagnosed vaginal bleeding (Lupron
Anaphylaxis occurs rarely. Diarrhea may Depot 3.75 mg and 11.25 mg). 22.5 mg,
cause rapid clinical deterioration. 30 mg, 45 mg Lupron Depot and Eligard
(all strengths) not indicated for use in
NURSING CONSIDERATIONS women. Cautions: History of psychiatric
BASELINE ASSESSMENT illness, QTc prolongation or medications
Obtain baseline CBC, LFT, renal func- that prolong QTc interval, preexisting
tion. Give as soon as possible, preferably cardiac disease, chronic alcohol use, ste-
within 1 hr, for treatment of accidental roid therapy, seizures or medications that
overdosage of folic acid antagonists. decrease seizures threshold.
INTERVENTION/EVALUATION ACTION
Monitor for vomiting (may need to Inhibits gonadotropin secretion; pro-
change from oral to parenteral therapy). duces an initial increase in LH and FSH,

Canadian trade name Non-Crushable Drug High Alert drug


684 leuprolide
causing a transient increase in testoster- ADMINISTRATION/HANDLING
one (males) and estrone/estradione in b ALERT c May be carcinogenic, muta-
premenopausal women. Continuous ad- genic, teratogenic. Handle with extreme
ministration results in decreased levels of care during preparation/administration.
testosterone (male) and estrogen (fe-
males). Therapeutic Effect: Produces IM
pharmacologic castration, decreases • (Lupron Depot): Store at room
growth of abnormal prostate tissue in temperature. • Protect from light,
males; causes endometrial tissue to be- heat. • Do not freeze vials. • Re-
come inactive, atrophic in females; de- constitute only with diluent provided.
creases rate of pubertal development in Follow manufacturer’s instructions for
children with central precocious puberty. mixing. • Do not use needles less than
22 gauge; use syringes provided by the
PHARMACOKINETICS manufacturer (0.5-mL low-dose insu-
Rapidly, well absorbed after SQ admin- lin syringes may be used as an alterna-
istration. Absorbed slowly after IM ad- tive). • Administer immediately.
ministration. Protein binding: 43%–49%. • (Eligard): Refrigerate. • Allow to
Half-life: 3–4 hrs. warm to room temperature before re-
constitution. • Follow manufacturer’s
L LIFESPAN CONSIDERATIONS instructions for mixing. • Following re-
Pregnancy/Lactation: Depot: Con- constitution, administer within 30 min.
traindicated in pregnancy. May cause
spontaneous abortion. Children: Long- SQ
term safety not established. Elderly: No • (Lupron): Refrigerate vials. • In-
age-related precautions noted. jection appears clear, colorless. • Dis-
card if ­ discolored or precipitate
INTERACTIONS forms. • Administer into deltoid mus-
DRUG: QT interval–prolonging medi­ cle, anterior thigh, abdomen.
cations (e.g., amiodarone, azithro-
mycin, ceritinib, haloperidol, INDICATIONS/ROUTES/DOSAGE
moxifloxacin) may increase risk of QT Advanced Prostatic Carcinoma
interval prolongation, cardiac arrhythmias. IM: (Lupron Depot): ADULTS, ELDERLY:
HERBAL: None significant. FOOD: None 7.5 mg q1mo, 22.5 mg q3mos, 30 mg
known. LAB VALUES: May increase se- q4mos, or 45 mg q6mos.
rum prostatic acid phosphatase (PAP). SQ: (Eligard): ADULTS, ELDERLY: 7.5 mg
Initially increases, then decreases serum every mo, 22.5 mg q3mos, 30 mg q4mos,
testosterone. May increase serum ALT, AST, or 45 mg q6mos.
alkaline phosphatase, glucose, LDH, LDL, SQ: (Lupron): ADULTS, ELDERLY: 1 mg/
cholesterol, triglycerides. May decrease day.
platelets, WBC.
Endometriosis
AVAILABILITY (Rx) IM: (Lupron Depot): ADULTS, EL-
Injection Depot Formulation: (Eligard): DERLY: 3.75 mg/mo for up to 6 mos or
7.5 mg, 22.5 mg, 30 mg, 45 mg. (Lu- 11.25 mg q3mos for up to 2 doses.
pron Depot-Ped): 7.5 mg, 11.25 mg
Uterine Leiomyomata
(3-month), 11.25 (monthly), 15 mg, 30 IM: (with Iron [Lupron Depot]): ADULTS,
mg. (Lupron Depot): 3.75 mg, 11.25 mg, ELDERLY:3.75 mg/mo for up to 3 mos or
22.5 mg, 30 mg, 45 mg. Injection Solu- 11.25 mg as a single injection.
tion: 5 mg/mL.

underlined – top prescribed drug


levalbuterol 685
Precocious Puberty level or less within 2 wks, PAP within 4
IM: (Lupron Depot-Ped): CHILDREN wks. Question medical history as listed
WEIGHING MORE THAN 37.5 KG: 15 mg in Precautions. Offer emotional support.
q1mo. WEIGHING 25 KG TO 37.5 KG: 11.25
mg q1mo. WEIGHING 25 KG OR LESS: 7.5 INTERVENTION/EVALUATION
mg q1mo. Titrate dose upward by 3.75 Monitor for arrhythmias, palpitations. As-
mg/mo if down regulation not achieved. sess for peripheral edema. Assess sleep
LUPRON DEPOT-PED (3 MOS): 11.25 mg or pattern. Monitor for visual difficulties. As-
30 mg q12wks. sist with ambulation if dizziness occurs.
SQ: (Lupron): CHILDREN: Initially, 50 mcg/ Offer antiemetics if nausea occurs.
kg/day. Titrate upward by 10 mcg/kg/day PATIENT/ FAMILY TEACHING
if down regulation is not achieved.
• Hot flashes tend to decrease during
Dosage in Renal/Hepatic Impairment continued therapy. • Temporary exac-
No dose adjustment. erbation of signs/symptoms of disease
may occur during first few wks of ther-
SIDE EFFECTS apy. • Use contraceptive measures. •
Frequent: Hot flashes (ranging from Report persistent, regular menstruation;
mild flushing to diaphoresis), migraines, pregnancy. • Avoid tasks that require
hyperhidrosis. Females: Amenorrhea, alertness, motor skills until response to L
spotting. Occasional: Arrhythmias, palpi- drug is established (potential for dizzi-
tations, blurred vision, dizziness, edema, ness).
headache, burning, pruritus, swelling at in-
jection site, nausea, insomnia, weight gain.
Females: Deepening voice, hirsutism,
decreased libido, increased breast ten-
levalbuterol
derness, vaginitis, altered mood. Males: lee-val-bue-ter-ole
Constipation, decreased testicle size, gyne- (Xopenex, Xopenex HFA, Xopenex
comastia, impotence, decreased appetite, Concentrate)
angina. Rare: Males: Thrombophlebitis. Do not confuse Xopenex with
ADVERSE EFFECTS/TOXIC Xanax.
REACTIONS uCLASSIFICATION
Occasionally, signs/symptoms of pros- PHARMACOTHERAPEUTIC: Beta 2
tatic carcinoma worsen 1–2 wks after agonist. CLINICAL: Bronchodilator.
initial dosing (subsides during continued
therapy). Increased bone pain and, less
frequently, dysuria, hematuria, weakness, USES
paresthesia of lower extremities may be Treatment, prevention of bronchospasm
noted. MI, pulmonary embolism occur due to reversible obstructive airway dis-
rarely. ease (e.g., asthma, bronchitis, emphy-
sema). OFF-LABEL: Treatment of asthma
NURSING CONSIDERATIONS
in children younger than 4 yrs of age.
BASELINE ASSESSMENT
Question for possibility of pregnancy
PRECAUTIONS
before initiating therapy. Obtain serum Contraindications: History of hypersen-
testosterone, prostatic acid phosphates sitivity to albuterol or levalbuterol. Cau-
(PAP) periodically during therapy. Se- tions: Cardiovascular disorders (cardiac
rum testosterone, PAP should increase arrhythmias, HF), seizures, hypertension,
during first wk of therapy. Serum testos- hyperthyroidism, diabetes, glaucoma,
terone then should decrease to baseline hypokalemia.

Canadian trade name Non-Crushable Drug High Alert drug


686 levalbuterol

ACTION orless. • Do not mix with other medi-


Stimulates beta2-adrenergic receptors cations. • Concentrated solution (1.25
in lungs, resulting in relaxation of bron- mg in 0.5 mL) should be diluted with 2.5
chial smooth muscle. Therapeutic Ef- mL 0.9% NaCl prior to use. • Give over
fect: Relieves bronchospasm, reduces 5–15 min.
airway resistance.
Inhalation
PHARMACOKINETICS • Shake well before inhalation. • Prime
before initial use or if not used for more
Route Onset Peak Duration
than 3 days. • Following first inhalation,
Inhalation 5–10 min 1.5 hrs 5–6 hrs wait 2 min before inhaling second dose
Nebulization 10–17 min 1.5 hrs 5–8 hrs
(allows for deeper bronchial penetra-
Half-life: 3.3–4 hrs. tion). • Rinsing mouth with water im-
mediately after inhalation prevents mouth/
LIFESPAN CONSIDERATIONS throat dryness.
Pregnancy/Lactation: Crosses placenta.
Unknown if distributed in breast milk.
INDICATIONS/ROUTES/DOSAGE
Pregnancy Category C. Children: Safety Treatment/Prevention of Bronchospasm
and efficacy not established in pts younger Nebulization: ADULTS, ELDERLY, CHIL-
L than 12 yrs. Elderly: Lower initial dosages DREN 12 YRS AND OLDER: Initially, 0.63 mg
recommended. 3 times/day 6–8 hrs apart. May increase to
1.25 mg 3 times/day with close monitor-
INTERACTIONS ing. CHILDREN 5–11 YRS: Initially, 0.31 mg
DRUG: Beta blockers (e.g., carvedilol, 3 times/day. Maximum: 0.63 mg 3 times/
metoprolol) antagonize effects; may day. CHILDREN 4 YRS OR YOUNGER: 0.31–
produce severe bronchospasm. MAOIs 1.25 mg q4–6h as needed.
(e.g., phenelzine, tranylcypromine), Inhalation: ADULTS, ELDERLY, CHILDREN 4
tricyclic antidepressants (e.g., ami- YRS AND OLDER: 1–2 inhalations q4–6h.
triptyline, desipramine) may poten-
Acute Asthma Exacerbation
tiate cardiovascular effects. Diuretics
Nebulization: ADULTS, ELDERLY, CHILDREN
(e.g., furosemide, HCTZ) may increase
12 YRS AND OLDER: 1.25–2.5 mg q20min for
hypokalemia. Linezolid may enhance the
3 doses, then 1.25–5 mg q1–4h as needed.
hypertensive effect. May increase adverse
CHILDREN YOUNGER THAN 12 YRS: 0.075
effects of loxapine. HERBAL: None sig-
mg/kg (minimum dose: 1.25 mg) q20min
nificant. FOOD: None known. LAB VAL-
for 3 doses, then 0.075–0.15 mg/kg (Maxi-
UES: May decrease serum potassium.
mum: 5 mg dose) q1–4h as needed.
AVAILABILITY (Rx) Inhalation: ADULTS, ELDERLY, CHILDREN
12 YRS AND OLDER: 4–8 puffs q20min
Inhalation Aerosol: 45 mcg/activation.
for up to 4 hrs, then q1–4h. CHILDREN
Solution for Nebulization: 0.31 mg in
YOUNGER THAN 12 YRS: 4–8 puffs q20min
3-mL vials, 0.63 mg in 3-mL vials, 1.25
for 3 doses, then q1–4h.
mg in 3-mL vials, 1.25 mg in 0.5-mL vials.
Dosage in Renal/Hepatic Impairment
ADMINISTRATION/HANDLING
No dose adjustment.
Nebulization
• No diluent necessary. • Protect from SIDE EFFECTS
light, excessive heat. Store at room tem- Occasional (11%–4%): Nervousness, tre­
perature. • Once foil is opened, use mor, rhinitis, flu-like illness. Rare (less
within 2 wks. • Use within 1 wk and than 3%): Tachycardia, dizziness, anxiety,
protect from light after removal from viral infection, dyspepsia, dry mouth,
pouch • Discard if solution is not col- headache, chest pain.
underlined – top prescribed drug
levETIRAcetam 687

ADVERSE EFFECTS/TOXIC USES


REACTIONS Adjunctive therapy in treatment of partial-
Excessive sympathomimetic stimulation onset, myoclonic, and/or primary gener-
may produce palpitations, premature heart alized tonic-clonic seizures.
contraction, tachycardia, chest pain, slight
increase in B/P followed by substantial PRECAUTIONS
decrease, chills, diaphoresis, blanching of Contraindications: Hypersensitivity to
skin. Too-frequent or excessive use may de- levETIRAcetam. Cautions: Renal impair-
crease bronchodilating effectiveness, lead ment, pts with depression at high risk for
to severe, paradoxical bronchoconstriction. suicide.

NURSING CONSIDERATIONS ACTION


Exact mechanism unknown. May inhibit
BASELINE ASSESSMENT
voltage-dependent calcium channels,
Assess lung sounds, pulse, B/P, oxygen facilitate GABA inhibitory transmission,
saturation. Note color, amount of sputum. reduce potassium current, or bind to
INTERVENTION/EVALUATION synaptic proteins that modulate neu-
rotransmitter release. Therapeutic Ef-
Monitor rate, depth, rhythm, type of fect: Prevents seizure activity.
respiration; quality/rate of pulse, ECG, L
serum potassium, ABG determinations. PHARMACOKINETICS
Assess lung sounds for wheezing (bron- Rapidly, completely absorbed follow-
choconstriction). Observe for paradoxi- ing PO administration. Protein binding:
cal bronchospasm. less than 10%. Metabolized primarily
PATIENT/ FAMILY TEACHING by enzymatic hydrolysis. Primarily ex-
• Increase fluid intake (decreases lung creted in urine as unchanged drug. Half-
secretion viscosity). • Rinsing mouth life: 6–8 hrs.
with water immediately after inhalation LIFESPAN CONSIDERATIONS
may prevent mouth/throat dryness. Pregnancy/Lactation: Distributed
• Avoid excessive use of caffeine deriva- in breast milk. Breastfeeding not rec-
tives (chocolate, coffee, tea, cola, cocoa). ommended. Children: Safety and ef-
• Report if palpitations, tachycardia, chest ficacy not established in children 4
pain, tremors, dizziness, headache occurs yrs or younger. Elderly: Age-related
or shortness of breath is not relieved. renal impairment may require dosage
adjustment.
INTERACTIONS
levETIRAcetam DRUG: CNS depressants (e.g., al-
cohol, morphine, zolpidem)
lee-ve-tye-ra-se-tam may increase CNS depression.
(Keppra, Keppra XR, Spritam) HERBAL: Herbals with sedative prop-
Do not confuse Keppra with erties (e.g., chamomile, kava kava,
Kaletra, Keflex, or Keppra XR, valerian) may increase CNS depression.
or levETIRAcetam with levo- FOOD: None known. LAB VALUES: May
FLOXacin. decrease Hgb, Hct, RBC, WBC.
uCLASSIFICATION
AVAILABILITY (Rx)
PHARMACOTHERAPEUTIC: Pyrroli- Injection, Solution: 100 mg/mL. Oral
dine derivative. CLINICAL: Anticon- Solution: 100 mg/mL. Tablets: 250 mg,
vulsant. 500 mg, 750 mg, 1,000 mg.

Canadian trade name Non-Crushable Drug High Alert drug


688 levETIRAcetam

Tablets, Extended-Release: 500 mg, dose. Maximum: 1,500 mg twice daily.


750 mg. Tablets (ODT): 250 mg, 500 mg, 20–40 KG: 250 mg twice daily. May increase
750 mg, 1,000 mg. q2wks by 250 mg/dose. Maximum: 750
mg twice daily. CHILDREN 6 MOS TO YOUNGER
ADMINISTRATION/HANDLING THAN 4 YRS: (Oral Solution): 20 mg/kg/
IV day in 2 divided doses. May increase q2wks
by 10 mg/kg/dose. Maximum: 50 mg/kg/
Rate of infusion • Infuse over 15 min. day in 2 divided doses. CHILDREN 1 MO TO
Reconstitution • Dilute with 100 YOUNGER THAN 6 MOS: (Oral Solution): 14
mL 0.9% NaCl or D5W. mg/kg/day in 2 divided doses. May increase
Storage • Store at room tempera- q2wks by 7 mg/kg/dose. Maximum: 42
ture. • Stable for 24 hrs following mg/kg/day in 2 divided doses.
­dilution.
PO Myoclonic Seizures
• Give without regard to food. • Oral PO, IV: CHILDREN 16 YRS AND OLDER: (Im-
Solution: Use a calibrated measuring de- mediate-Release Tablets, Oral Solu-
vice. • Tablet (immediate-release, tion, Tablets for Oral Suspension):
extended-release): Administer tablet Initially, 500 mg q12h. May increase by
whole; do not cut, break, or crush. • Tab- 1,000 mg/day q2wks. Maximum: 3,000
L let (ODT): Place whole tablet on tongue mg/day in 2 divided doses. CHILDREN 6–15
and follow with sip of liquid. Swallowing YRS: Initially, 10 mg/kg twice daily. May in-
allowed only after tablet has disinte- crease by 10 mg/kg/dose q2wks up to rec-
grated. • Use oral solution for pts weigh- ommended dose of 30 mg/kg twice daily.
ing 20 kg or less. • Use tablets or oral
solution for pts weighing more than 20 kg. Tonic-Clonic Seizures
PO, IV: ADULTS, ELDERLY, CHILDREN 16
IV COMPATIBILITIES YRS AND OLDER: (Immediate-Release
DiazePAM (Valium), LORazepam (Ati- Tablets, Oral Solution, Tablets for
van), valproate (Depacon). Oral Suspension): Initially, 500 mg
twice daily. May increase by 1,000 mg/day
INDICATIONS/ROUTES/DOSAGE q2wks up to recommended dose of 1,500
Partial-Onset Seizures mg 2 times/day. CHILDREN 6–15 YRS: Ini-
IV/PO: ADULTS, ELDERLY, CHILDREN 17 tially, 10 mg/kg twice daily. May increase
YRS AND OLDER: (Immediate-Release by 20 mg/kg/day q2wks up to recom-
Tablets, Oral Solution, Tablets for mended dose of 30 mg/kg 2 times/day.
Oral Suspension): Initially, 500 mg
Dosage in Renal Impairment
q12h. May increase by 1,000 mg/day
Dosage is modified based on creatinine
q2wks. Maximum: 3,000 mg/day in
clearance. Note: CrCl less than 50 mL/
2 divided doses. (Extended-Release
min: Not recommended with Keppra XR.
Tablets): 1,000 mg once daily. May
Dosage Dosage
increase in increments of 1,000 mg/
Creatinine (Immediate- (Extended-
day q2wks. Maximum: 3,000 mg once
Clearance Release, IV) Release)
daily.
IV/PO: CHILDREN 4–16 YRS: (Oral Solu- Greater than 500–1,500 mg 1,000–3,000
80 mL/min: q12h mg q24h
tion, Tablets): 20 mg/kg/day in 2 divided
50–80 mL/ 500–1,000 mg 1,000–2,000
doses. May increase q2wks by 10 mg/ min: q12h mg q24h
kg/dose up to 60 mg/kg/day in 2 divided 30–49 mL/ 250–750 mg 500–1,500
doses. Maximum: 3,000 mg/day. (Tab- min: q12h mg q24h
lets): WEIGHING MORE THAN 40 KG: 500 mg Less than 30 250–500 mg 500–1,000
twice daily. May increase q2wks by 500 mg/ mL/min: q12h mg q24h

underlined – top prescribed drug


levoFLOXacin 689
Dosage Dosage changes. Assist with ambulation if dizzi-
Creatinine (Immediate- (Extended- ness occurs.
Clearance Release, IV) Release)
PATIENT/ FAMILY TEACHING
End-stage 500–1,000 mg NA
renal dis- q24h; after di- • Drowsiness usually diminishes with
ease using alysis, a 250– continued therapy. • Avoid tasks that
dialysis: to 500–mg require alertness, motor skills until re-
supplemental sponse to drug is established. • Avoid
dose is rec- alcohol. • Do not abruptly discontinue
ommended
CRRT 250–750 mg
medication (may precipitate sei-
q12h zures). • Strict maintenance of drug
therapy is essential for seizure con-
trol. • Report mood swings, hostile
Dosage in Hepatic Impairment behavior, suicidal ideation, unusual
No dose adjustment. changes in behavior.
SIDE EFFECTS
Frequent (15%–10%): Drowsiness, as-
thenia, headache, infection. Occasional levoFLOXacin
(9%–3%): Dizziness, pharyngitis, pain, L
depression, anxiety, vertigo, rhinitis, lee-voe-flox-a-sin
anorexia. Rare (less than 3%): Amnesia, (Iquix, Levaquin, Quixin)
emotional lability, cough, sinusitis, an- j BLACK BOX ALERT jMay
orexia, diplopia. increase risk of tendonitis, tendon
rupture. (Risk increased with
ADVERSE EFFECTS/TOXIC concurrent corticosteroids, organ
REACTIONS transplant, pts older than 60 yrs.)
May exacerbate myasthenia gravis.
Acute psychosis, agitation, delirium,
Do not confuse Levaquin with
impulsivity have been reported. Sudden
Levoxyl, Levsin/SL, or Lovenox,
discontinuance increases risk of seizure
or levoFLOXacin with levETI-
activity. Serious dermatological reactions,
RAcetam or levothyroxine.
including Stevens-Johnson syndrome and
toxic epidermal necrolysis, have been uCLASSIFICATION
reported.
PHARMACOTHERAPEUTIC: Fluoro-
quinolone. CLINICAL: Antibiotic.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT USES
Review history of seizure disorder (in- Treatment of susceptible infections due to
tensity, frequency, duration, LOC). Initi- S. pneumoniae, S. aureus, E. faecalis,
ate seizure precautions. Question prior H. influenzae, M. catarrhalis, Serratia
hypersensitivity reaction. Obtain renal marcescens, K. pneumoniae, E. coli, P.
function test. mirabilis, P. aeruginosa, C. pneumoniae,
Legionella pneumophila, Mycoplasma
INTERVENTION/EVALUATION pneumoniae, including acute bacterial
Observe for recurrence of seizure activ- exacerbation of chronic bronchitis, acute
ity. Assess for clinical improvement (de- bacterial sinusitis, community-acquired
crease in intensity/frequency of seizures). pneumonia, nosocomial pneumonia,
Monitor renal function tests. Observe for complicated and uncomplicated UTI,
suicidal ideation, depression, behavioral acute pyelonephritis, complicated and
uncomplicated mild to moderate skin/

Canadian trade name Non-Crushable Drug High Alert drug


690 levoFLOXacin
skin structure infections, prostatitis. In- ibuprofen, ketorolac, naproxen)
halation anthrax (postexposure); plague. may increase risk of CNS stimulation,
Ophthalmic: Treatment of superficial seizures. Medications that prolong
infections to conjunctiva (0.5%), cornea QT interval (e.g., amiodarone, halo-
(1.5%). OFF-LABEL: Urethritis, traveler’s peridol, sotalol) may increase risk
diarrhea, diverticulitis, enterocolitis, Le- of arrhythmias. May increase effects of
gionnaire’s disease, peritonitis. Treatment warfarin. HERBAL: None significant.
of prosthetic joint infection. FOOD: None known. LAB VALUES: May
alter serum glucose.
PRECAUTIONS
Contraindications: Hypersensitivity to AVAILABILITY (Rx)
levoFLOXacin, other fluoroquinolones. Infusion Premix: 250 mg/50 mL, 500
Cautions: Known or suspected CNS disor- mg/100 mL, 750 mg/150 mL. Injection,
ders, seizure disorder, renal impairment, Solution: 25 mg/mL. Ophthalmic Solu-
bradycardia, rheumatoid arthritis, elderly, tion: 0.5%. Oral Solution: 25 mg/mL.
hypokalemia, hypomagnesemia, myasthe- Tablets: 250 mg, 500 mg, 750 mg.
nia gravis, severe cerebral arteriosclero-
sis, prolonged QT interval, medications ADMINISTRATION/HANDLING
that potentiate QT interval prolongation, IV
L diabetes, pts at risk for tendon rupture,
tendonitis (e.g., renal failure, concomitant Reconstitution • For infusion using
use of corticosteroids, organ transplant single-dose vial, withdraw desired
recipient, rheumatoid arthritis, elderly, amount (10 mL for 250 mg, 20 mL for
strenuous physical activity or exercise). 500 mg). Dilute each 10 mL (250 mg)
with minimum 40 mL 0.9% NaCl, D5W,
ACTION providing a concentration of 5 mg/mL.
Inhibits DNA enzyme gyrase in suscep- Rate of administration • Administer
tible microorganisms, interfering with no less than 60 min for 250 mg or 500
bacterial cell replication, repair. Thera- mg; 90 min for 750 mg.
peutic Effect: Bactericidal. Storage • Available in single-dose 20-
mL (500-mg) vials and premixed with
PHARMACOKINETICS D5W, ready to infuse. • Diluted vials
Well absorbed after PO, IV administra- stable for 72 hrs at room temperature,
tion. Protein binding: 50%. Widely dis- 14 days if refrigerated.
tributed. Excreted unchanged in urine.
Partially removed by hemodialysis. Half- PO
life: 6–8 hrs. • Do not administer antacids (alumi-
num, magnesium), sucralfate, iron or
LIFESPAN CONSIDERATIONS multivitamin preparations with zinc within
Pregnancy/Lactation: Distributed 2 hrs of administration (significantly re-
in breast milk. Avoid use in pregnancy. duces absorption). • Give tablets with-
Children: Safety and efficacy not es- out regard to food. • Give oral solution
tablished. Elderly: Age-related re- 1 hr before or 2 hrs after meals.
nal impairment may require dosage Ophthalmic
adjustment. • Place a gloved finger on lower eyelid
INTERACTIONS and pull out until a pocket is formed
between eye and lower lid. • Place
­
DRUG: Antacids; calcium, magne- prescribed number of drops into
­
sium, iron preparations; sucralfate, pocket. • Instruct pt to close eye gently
zinc decrease absorption. NSAIDs (e.g., (so that medication will not be squeezed

underlined – top prescribed drug


levoFLOXacin 691
out of the sac) and to apply digital pres- Creatinine
sure to lacrimal sac for 1–2 min to mini- Clearance Dosage
mize systemic absorption. 50–80 mL/min No change
20–49 mL/min Initially, 750 mg, then
IV INCOMPATIBILITIES 750 mg q48h
Furosemide (Lasix), heparin, insulin, ni- 10–19 mL/min Initially, 750 mg, then
500 mg q48h
troglycerin, propofol (Diprivan). Dialysis 500 mg q48h (adminis-
ter after dialysis on
IV COMPATIBILITIES dialysis days)
Dexmedetomidine (Precedex), DOBUTa- Continuous
mine (Dobutrex), DOPamine (Intropin), ­Renal Replace-
fentaNYL (Sublimaze), lidocaine, (Ati- ment Therapy
van), magnesium, morphine. CVVH 500–750 mg once,
then 250 mg q24h
INDICATIONS/ROUTES/ CVVHD 500–750 mg once,
DOSAGE then 250–500 mg q24h
CVVHDT 500–750 mg once,
Usual Dosage Range then 250–750 mg q24h
PO, IV: ADULTS, ELDERLY:250–500 mg
q24h; 750 mg q24h for severe or com-
plicated infections. Dosage in Hepatic Impairment L
No dose adjustment.
Bacterial Conjunctivitis
Ophthalmic: ADULTS, ELDERLY, CHILDREN SIDE EFFECTS
1 YR AND OLDER: (Quixin 0.5%): 1–2 Occasional (3%–1%): Diarrhea, nau-
drops q2h for 2 days while awake (up to sea, abdominal pain, dizziness, drowsi-
8 times/day), then 1–2 drops q4h while ness, headache. Ophthalmic: Local
awake up to 4 times/day. burning/discomfort, margin crusting,
crystals/scales, foreign body sensation,
Dosage in Renal Impairment ocular itching, altered taste. Rare (less
Normal renal function dosage of 250 mg/ than 1%): Flatulence; pain, inflammation,
day: swelling in calves, hands, shoulder; chest
Creatinine pain, difficulty breathing, palpitations,
Clearance Dosage edema, tendon pain. Ophthalmic: Cor-
20–49 mL/min No change neal staining, keratitis, allergic reaction,
10–19 mL/min 250 mg initially, eyelid swelling, tearing, reduced visual
then 250 mg q48h acuity.
Normal renal function dosage of 500 ADVERSE EFFECTS/TOXIC
mg/day: REACTIONS
Creatinine
Antibiotic-associated colitis, other su-
Clearance Dosage
perinfections (abdominal cramps, se-
50–80 mL/min No change vere watery diarrhea, fever) may occur.
20–49 mL/min 500 mg initially,
Superinfection (genital/anal pruritus,
then 250 mg q24h
10–19 mL/min 500 mg initially, ulceration/changes in oral mucosa,
then 250 mg q48h moderate to severe diarrhea) may occur
from altered bacterial balance in GI tract.
For pts undergoing dialysis, 500 mg ini- Hypersensitivity reactions, including
tially, then 250 mg q48h. photosensitivity (rash, pruritus, blisters,
Normal renal function dosage of 750 edema, sensation of burning skin), have
mg/day: occurred in pts receiving fluoroquino-
lones. May increase risk of tendonitis,

Canadian trade name Non-Crushable Drug High Alert drug


692 levothyroxine
tendon rupture, peripheral neuropathy; trouble sleeping. • Treatment may
CNS effects including agitation, anxiety, cause heart problems such as low heart
confusion, depression, dizziness, halluci- rate, palpitations; permanent nerve dam-
nations, nightmares, paranoia, tremors, age such as burning, numbness, tingling,
vertigo. May exacerbate muscle weakness weakness. • Do not take aluminum- or
in pts with myasthenia gravis. magnesium-containing antacids, multivi-
tamins, zinc or iron products at least 2
NURSING CONSIDERATIONS hrs before or 6 hrs after dose. • Drink
plenty of fluids.
BASELINE ASSESSMENT
Question for hypersensitivity to levoFLOX-
acin, other fluoroquinolones. Question
history as listed in Precautions. Receive
levothyroxine
full medication history, and screen for in- lee-voe-thy-rox-een
teractions, esp. medications that prolong (Eltroxin , Euthyrox, Levoxyl,
QT interval. Obtain baseline ECG. Synthroid, Tirosint, Unithroid)
INTERVENTION/EVALUATION j BLACK BOX ALERT jIneffec-
tive, potentially toxic for weight
Monitor serum glucose, renal function, reduction. High doses increase risk
L LFT. Monitor daily pattern of bowel ac- of serious, life-threatening toxic
tivity, stool consistency. Promptly report effects, especially when used with
hypersensitivity reaction: skin rash, urti- some anorectic drugs.
caria, pruritus, photosensitivity. Be alert Do not confuse levothyroxine
for superinfection: fever, vomiting, diar- with levoFLOXacin or liothy-
rhea, anal/genital pruritus, oral mucosal ronine, or Synthroid with
changes (ulceration, pain, erythema). Symmetrel.
Monitor for muscle weakness, voice dys-
tonia in pts with myasthenia gravis; pain, FIXED-COMBINATION(S)
swelling, bruising, popping of tendons. With liothyronine, T3(Thyrolar).
PATIENT/ FAMILY TEACHING uCLASSIFICATION
• It is essential to complete drug ther- PHARMACOTHERAPEUTIC: Synthetic
apy despite symptom improvement. Early isomer of thyroxine. CLINICAL: Thy-
discontinuation may result in antibacte- roid hormone (T4).
rial resistance or increase risk of recur-
rent infection. • Report any episodes of
diarrhea, esp. the first few mos after final USES
dose. Frequent diarrhea, fever, abdomi- PO: Treatment of hypothyroidism, pitu-
nal pain, blood-streaked stool may indi- itary thyroid-stimulating hormone (TSH)
cate infectious diarrhea, which may be suppression. IV: Myxedema coma. OFF-
contagious to others. • Severe allergic LABEL: Management of hemodynamically
reactions, such as hives, palpitations, unstable potential organ donors.
rash, shortness of breath, tongue swell-
ing, may occur. • Tendon inflamma- PRECAUTIONS
tion/swelling, tendon rupture may occur; Contraindications: Hypersensitivity to le-
report bruising, pain, swelling in tendon vothyroxine. Acute MI, untreated subclin-
areas or snapping, popping of ten- ical or overt thyrotoxicosis, uncorrected
dons. • Immediately report nervous adrenal insufficiency. Capsule: Inability
system problems such as anxiety, confu- to swallow capsules. Cautions: Elderly
sion, dizziness, nervousness, nightmares, pts, angina pectoris, hypertension,
thoughts of suicide, seizures, tremors, other cardiovascular disease, adrenal

underlined – top prescribed drug


levothyroxine 693
insufficiency, myxedema, diabetes mel- ADMINISTRATION/HANDLING
litus and insipidus, swallowing disorders. b ALERT c Do not interchange brands
(known issues with bioequivalence be-
ACTION
tween manufacturers).
Converts to T3, then binds to thyroid
receptor proteins exerting metabolic ef- IV
fects through control of DNA transcrip- Reconstitution • Reconstitute 200-
tion and protein synthesis. Therapeutic mcg or 500-mcg vial with 5 mL 0.9% NaCl
Effect: Involved in normal metabolism, to provide concentration of 40 or 100
growth and development. Increases basal mcg/mL, respectively; shake until clear.
metabolic rate, enhances gluconeogen- Rate of administration • Use imme-
esis, stimulates protein synthesis. diately; discard unused portions. • Give
each 100 mcg or less over 1 min.
PHARMACOKINETICS Storage • Store vials at room temper-
Variable, incomplete absorption from ature.
GI tract. Protein binding: greater than
99%. Widely distributed. Deiodinated in PO
peripheral tissues, minimal metabolism • Administer in the morning on an
in liver. Eliminated by biliary excretion. empty stomach, 30 min before
Half-life: 6–7 days. food. • Administer before breakfast to L
prevent insomnia. • Tablets may be
LIFESPAN CONSIDERATIONS crushed. • Take 4 hrs apart from ant-
Pregnancy/Lactation: Does not cross acids, iron, calcium supplements.
placenta. Minimal distribution in breast
milk. Children: No age-related pre- IV INCOMPATIBILITIES
cautions noted. Caution in neonates Do not use or mix with other IV solutions.
in interpreting thyroid function tests.
Elderly: May be more sensitive to INDICATIONS/ROUTES/DOSAGE
thyroid effects; individualized dosage Note: Doses based on clinical response
recommended. and laboratory parameters. IV dose is
75–80% of oral dose once daily.
INTERACTIONS
DRUG: Cholestyramine, colestipol, Hypothyroidism
alu­minum- and magnesium-containing PO: ADULTS 60 YRS OR YOUNGER WITH-
antacids, calcium, iron may decrease OUT EVIDENCE OF CORONARY HEART DIS-
absorption (do not administer within 4 EASE: 1.6 mcg/kg/day as single daily
hrs). Estrogens may decrease therapeutic dose. Adjust dose by 12.5–25 mcg/day
effect. May enhance effects of oral antico- q3–6 wks. Usual maintenance: 100–125
agulants (e.g., warfarin). HERBAL: None mcg/day. ADULTS OLDER THAN 60 YRS
significant. FOOD: None known. LAB VAL- WITHOUT EVIDENCE OF CORONARY HEART
UES: None known. DISEASE: Initially, 25–50 mcg once daily.
ADULTS WITH CARDIAC DISEASE: Initially,
AVAILABILITY (Rx) 12.5–50 mcg/day. Adjust dose by 12.5–
13 mcg, 25 mcg,
Capsules: (Tirosint): 25 mcg/day at 6–8-wk intervals. CHILDREN
50 mcg, 75 mcg, 88 mcg, 100 mcg, 112 OLDER THAN 12 YRS, GROWTH AND PUBERTY
mcg, 125 mcg, 137 mcg, 150 mcg. In- INCOMPLETE: 2–3 mcg/kg/day. CHIL-
jection, Powder for Reconstitution: 100 DREN 6–12 YRS: 4–5 mcg/kg/day.
mcg, 200 mcg, 500 mcg. Tablets: 25 CHILDREN 1–5 YRS: 5–6 mcg/kg/day.
mcg, 50 mcg, 75 mcg, 88 mcg, 100 mcg, CHILDREN 6–12 MOS: 6–8 mcg/kg/day.
112 mcg, 125 mcg, 137 mcg, 150 mcg, CHILDREN 3–5 MOS: 8–10 mcg/kg/day.
175 mcg, 200 mcg, 300 mcg.

Canadian trade name Non-Crushable Drug High Alert drug


694 lidocaine
CHILDREN YOUNGER THAN 3 MOS: 10–15 brain maturation, accelerates bone age.
mcg/kg/day. Monitor thyroid function tests.

Myxedema Coma PATIENT/ FAMILY TEACHING


IV: ADULTS, ELDERLY: Initially, 200–400 • Do not discontinue drug therapy; re-
mcg, then 50–100 mcg once daily until placement for hypothyroidism is life-
able to tolerate PO administration. long. • Follow-up office visits, thyroid
function tests are essential. • Take
Pituitary Thyroid-Stimulating Hormone medication at the same time each day,
(TSH) Suppression preferably in the morning. • Monitor
PO: ADULTS, ELDERLY: Doses greater pulse for rate, rhythm; report irregular
than 2 mcg/kg/day usually required to rhythm or pulse rate over 100 beats/
suppress TSH below 0.1 milliunits/L. min. • Promptly report chest pain,
weight loss, anxiety, tremors, insom-
Dosage in Renal/Hepatic Impairment nia. • Children may have reversible
No dose adjustment. hair loss, increased aggressiveness dur-
ing first few mos of therapy. • Full
SIDE EFFECTS therapeutic effect may take 1–3 wks.
Occasional: Reversible hair loss at start
L of therapy in children. Rare: Dry skin, GI
intolerance, rash, urticaria, pseudotumor
cerebri, severe headache in children. lidocaine
ADVERSE EFFECTS/TOXIC lye-doe-kane
REACTIONS (Lidoderm, Xylocaine)
Excessive dosage produces signs/symptoms FIXED-COMBINATION(S)
of hyperthyroidism (weight loss, palpita-
tions, increased appetite, tremors, anxi- EMLA: lidocaine/prilocaine (an
ety, tachycardia, hypertension, headache, anesthetic): 2.5%/2.5%. Lidosite:
insomnia, menstrual irregularities). Car- lidocaine/EPINEPHrine (a sympa-
diac arrhythmias occur rarely. Long-term thomimetic): 10%/0.1%. Lidocaine
therapy may decrease bone mineral density. with EPINEPHrine: lidocaine/
EPINEPHrine (a sympathomimetic):
NURSING CONSIDERATIONS 2%/1:50,000, 1%/1:100,000, 1%/
1:200,000, 0.5%/1:200,000. Syn-
BASELINE ASSESSMENT éra: lidocaine/tetracaine (an anes-
Obtain baseline TSH, T3, T4, weight, vi- thetic): 70 mg/70 mg.
tal signs. Signs/symptoms of diabetes,
diabetes insipidus, adrenal insufficiency, uCLASSIFICATION
hypopituitarism may become intensified. PHARMACOTHERAPEUTIC: Amide
Treat with adrenocortical steroids before anesthetic. CLINICAL: Class 1B anti-
thyroid therapy in coexisting hypothy- arrhythmic, anesthetic.
roidism and hypoadrenalism.
INTERVENTION/EVALUATION USES
Monitor pulse for rate, rhythm (report Antiarrhythmic: Rapid control of acute
pulse greater than 100 or marked in- ventricular arrhythmias following MI,
crease). Observe for tremors, anxiety. cardiac catheterization, cardiac surgery.
Assess appetite, sleep pattern. Children: Local anesthetic: Infiltration/nerve
(Undertreatment): May decrease in- block for dental/surgical procedures,
tellectual development, linear growth. childbirth. Topical anesthetic: Lo-
(Overtreatment): Adversely affects cal skin disorders (minor burns, insect
underlined – top prescribed drug
lidocaine 695
bites, prickly heat, skin manifestations LIFESPAN CONSIDERATIONS
of chickenpox, abrasions). Mucous Pregnancy/Lactation: Crosses pla-
membranes (local anesthesia of oral, centa. Distributed in breast milk. Chil-
nasal, laryngeal mucous membranes; dren: No age-related precautions noted.
local anesthesia of respiratory, urinary Elderly: More sensitive to adverse ef-
tracts; relief of discomfort of pruritus fects. Dose, rate of infusion should be
ani, hemorrhoids, pruritus vulvae). reduced. Age-related renal impairment
Dermal patch: Relief of chronic pain in may require dosage adjustment.
postherpetic neuralgia, allodynia (pain-
ful hypersensitivity). INTERACTIONS
PRECAUTIONS DRUG: Strong CYP3A4 inhibitors
(e.g., clarithromycin, ketoconazole,
Contraindications: Hypersensitivity to ritonavir), CYP1A2 inhibitors (e.g.,
lidocaine. Adams-Stokes syndrome, ciprofloxacin) may increase concentra-
hypersensitivity to amide-type local an- tion/effect. Strong CYP3A4 inducers
esthetics, supraventricular arrhythmias, (e.g., carBAMazepine, phenytoin,
Wolff-Parkinson-White syndrome. Severe rifAMPin) may decrease concentration/
degree of SA, AV, or intraventricular heart effect. HERBAL: St. John’s wort may de-
block (except in pts with functioning crease concentration/effect. FOOD: None
pacemaker). Cautions: Hepatic disease, known. LAB VALUES: IM lidocaine may L
marked hypoxia, severe respiratory increase creatine kinase (CK) level.
depression, hypovolemia, incomplete Therapeutic serum level: 1.5–6 mcg/
heart. History of malignant hyperthermia, mL; toxic serum level: greater than 6
shock, elderly pts, HF. mcg/mL.
ACTION AVAILABILITY (Rx)
Anesthetic: Inhibits conduction of nerve Cream, Topical: 4%. Infusion Premix:
impulses. Therapeutic Effect: Causes 0.4% (4 mg/mL in 250 mL, 500 mL);
temporary loss of feeling/sensation. An- 0.8% (8 mg/mL in 250 mL, 500 mL).
tiarrhythmic: Suppresses automaticity Injection, Solution: 0.5% (5 mg/mL),
of conduction tissue; increases electrical 1% (10 mg/mL), 2% (20 mg/mL). Jelly,
stimulation threshold of ventricle, His- Topical: 2%. Solution, Topical: 4%. So-
Purkinje system; and spontaneous depolar- lution, Viscous: 2%. Transdermal, Topi-
ization of ventricle during diastole. Blocks cal: (Lidoderm): 4%, 5%.
initiation/conduction of nerve impulses by
decreasing neuronal membrane’s perme- ADMINISTRATION/HANDLING
ability to sodium ions. Therapeutic Ef- b ALERT c Resuscitative equipment,
fect: Inhibits ventricular arrhythmias. drugs (including O2) must always be
PHARMACOKINETICS readily available when administering li-
docaine by any route.
Route Onset Peak Duration
IV
IV 30–90 sec N/A 10–20 min
Local 2.5 min N/A 30–60 min b ALERT c Use only lidocaine without
­anesthetic preservative, clearly marked for IV use.
Completely absorbed after IV administra- Reconstitution • For IV infusion,
tion. Protein binding: 60%–80%. Widely prepare solution by adding 2 g to 250–
distributed. Metabolized in liver. Primar- 500 mL D5W or 0.9% NaCl to provide
ily excreted in urine. Minimally removed concentration of 8 mg/mL or 4 mg/mL,
by hemodialysis. Half-life: 1–2 hrs. respectively. • Commercially available
preparations of 0.4% and 0.8% may be

Canadian trade name Non-Crushable Drug High Alert drug


696 lidocaine
used for IV infusion. Maximum con- CHILDREN, INFANTS: Initially, 1 mg/kg
centration: 4 g/250 mL (16 mg/mL). (Maximum: 100 mg). May repeat sec-
Rate of administration • For IV ond dose of 0.5–1 mg/kg if start of infusion
push, use 1% (10 mg/mL) or 2% (20 longer than 15 min. Maintenance: 20–
mg/mL). • Administer IV push at rate 50 mcg/kg/min as IV infusion.
of 25–50 mg/min. • Administer for IV
infusion at rate of 1–4 mg/min (1–4 Local Anesthesia
mL); use volume control IV set. Infiltration, nerve block: ADULTS: Lo-
Storage • Store premix solutions at cal anesthetic dosage varies with proce-
room temperature. dure, degree of anesthesia, vascularity,
duration. Maximum: 4.5 mg/kg or 300
Topical mg. Do not repeat within 2 hrs.
• Not for ophthalmic use. • For skin
disorders, apply directly to affected area Topical Local Anesthesia
or put on gauze or bandage, which is Topical: ADULTS, ELDERLY: Apply to af-
then applied to the skin. • For mucous fected areas as needed.
membrane use, apply to desired area per
Treatment of Localized Pain
manufacturer’s insert. • Administer
b ALERT c Transdermal patch may
lowest dosage possible that still provides
anesthesia. contain conducting metal (e.g., alumi-
L num). Remove patch prior to MRI.
Dermal Patch Topical: (Dermal Patch): ADULTS, EL-
Avoid exposing to external heat source. DERLY: Apply to intact skin over most
Patch should not get wet (do not wear painful area. Maximum: Up to 3
while bathing/swimming). Patch may be patches at a time for up to 12 hrs in a
cut to appropriate size. 24-hr period.

IV INCOMPATIBILITIES Dosage in Renal Impairment


Amphotericin B complex (Abelcet, AmBi- No dose adjustment.
some, Amphotec). Dosage in Hepatic Impairment
IV COMPATIBILITIES Use caution.
Amiodarone (Cordarone), calcium glu- SIDE EFFECTS
conate, dexmedetomidine (Precedex), CNS effects generally dose-related and
digoxin (Lanoxin), dilTIAZem (Cardi- of short duration. Occasional: Infiltra-
zem), DOBUTamine (Dobutrex), DO- tion/nerve block: Pain at injection site.
Pamine (Intropin), enalapril (Vasotec), Topical: Burning, stinging, tenderness at
furosemide (Lasix), heparin, insulin, application site. Rare: Generally associ-
nitroglycerin, potassium chloride. ated with high dose: Drowsiness, dizzi-
INDICATIONS/ROUTES/DOSAGE ness, disorientation, light-headedness,
tremors, apprehension, euphoria, sensa-
Ventricular Arrhythmias tion of heat, cold, numbness; blurred or
IV: ADULTS, ELDERLY: Initially, 1–1.5 mg/ double vision, tinnitus, nausea.
kg. Refractory ventricular tachycardia,
fibrillation: Repeat dose at 0.5–0.75 mg/ ADVERSE EFFECTS/TOXIC
kg q10–15min after initial dose for a maxi- REACTIONS
mum of 3 doses. Total dose not to exceed Serious adverse reactions to lidocaine
3 mg/kg. Follow with continuous infusion are uncommon, but high dosage by any
(1–4 mg/min) after return of circula- route may produce cardiovascular de-
tion. Reappearance of arrhythmia during pression, bradycardia, hypotension, ar-
infusion: 0.5 mg/kg, reassess infusion. rhythmias, heart block, cardiovascular

underlined – top prescribed drug


linaclotide 697
collapse, cardiac arrest. Potential for
malignant hyperthermia, CNS toxicity linaclotide
may occur, esp. with regional anesthesia
use, progressing rapidly from mild side lin-a-kloe-tide
effects to tremors, drowsiness, seizures, (Constella , Linzess)
vomiting, respiratory depression. Methe- j BLACK BOX ALERT jContrain-
moglobinemia (evidenced by cyanosis) dicated in pediatric pts 6 yrs of age
and younger. Avoid use in pediatric
has occurred following topical applica- patients 7 yrs through 17 yrs old.
tion of lidocaine for teething discomfort
and laryngeal anesthetic spray. uCLASSIFICATION

NURSING CONSIDERATIONS PHARMACOTHERAPEUTIC: Gua-


nylate cyclase-C (cGMP) agonist.
BASELINE ASSESSMENT CLINICAL: GI agent.
Question for hypersensitivity to lidocaine,
amide anesthetics. Obtain baseline B/P,
pulse, respiratory rate, ECG, serum elec- USES
trolytes. Treatment of irritable bowel syndrome
with constipation (IBS-C), chronic idio-
INTERVENTION/EVALUATION
pathic constipation (CIC) in adults. L
Monitor ECG, vital signs closely during and
following drug administration for cardiac PRECAUTIONS
performance. If ECG shows arrhythmias, Contraindications: Hypersensitivity to
prolongation of PR interval or QRS com- linaclotide. Pediatric patients 6 yrs and
plex, inform physician immediately. Assess younger, known or suspected mechani-
pulse for rhythm, rate, quality. Assess B/P cal GI obstruction. Cautions: Diarrhea.
for evidence of hypotension. Monitor for
therapeutic serum level (1.5–6 mcg/mL). ACTION
For lidocaine given by all routes, monitor Binds on the luminal surface of GI epithe-
vital signs, LOC. Drowsiness should be lium. Increases cGMP, which stimulates
considered a warning sign of high serum chloride and bicarbonate into intestinal
levels of lidocaine. Therapeutic serum lumen. Therapeutic Effect: Increases
level: 1.5–6 mcg/mL; toxic serum level: intestinal fluid, accelerates transit.
greater than 6 mcg/mL.
PHARMACOKINETICS
PATIENT/ FAMILY TEACHING
Metabolized within GI tract. Minimal dis-
• Local anesthesia: Due to loss of feel- tribution beyond GI tissue. Minimal sys-
ing/sensation, protective measures may be temic absorption. Half-life: N/A.
needed until anesthetic wears off (no am-
bulation, including special positions for LIFESPAN CONSIDERATIONS
some regional anesthesia). • Oral mu- Pregnancy/Lactation: Unknown if dis­
cous membrane anesthesia: Do not tributed in breast milk. Children: Avoid
eat, drink, chew gum for 1 hr after applica- use in pediatric pts 7 yrs through 17 yrs.
tion (swallowing reflex may be impaired, Contraindicated in pediatric pts 6 yrs and
increasing risk of aspiration; numbness of younger. Elderly: No age-related precau-
tongue, buccal mucosa may lead to bite tions noted.
trauma). • IV infusions: Report dizzi-
ness, numbness, double vision, nausea, INTERACTIONS
pain/burning, respiratory difficulty. DRUG: None significant. HERBAL: None
• Topical: Report irritation, pain, numb- significant. FOOD: None known. LAB
ness, swelling, blurred vision, tinnitus, re- VALUES: None significant.
spiratory difficulty.
Canadian trade name Non-Crushable Drug High Alert drug
698 linagliptin

AVAILABILITY (Rx) (relief from bloating, cramping, urgency,


abdominal discomfort). Monitor daily
Capsules: 72 mcg, 145 mcg, 290 mcg.
bowel activity, stool consistency. Monitor
ADMINISTRATION/HANDLING serum electrolytes in pts with prolonged,
frequent, or excessive use of medication.
PO
• Give on empty stomach at least 30 min PATIENT/FAMILY TEACHING
prior to first meal of day. • Do not break • Institute measures to promote defeca-
or crush. • For pts with swallowing diffi- tion: increase fluid intake, exercise, high-
culty, capsule may be opened and sprinkled fiber diet. • Report new/worsening
on applesauce or into 30 mL bottled water. ­episodes of abdominal pain, severe diar-
rhea. • Do not break, crush, or open
INDICATIONS/ROUTES/DOSAGE capsule. Take whole.
Irritable Bowel Syndrome with
Constipation
PO: ADULTS 18 YRS AND OLDER, EL-
290 mcg once daily.
DERLY:
linagliptin
Chronic Idiopathic Constipation
PO: ADULTS 18 YRS AND OLDER, EL- lin-a-glip-tin
L DERLY: 72–145 mcg once daily. (Tradjenta)
Do not confuse linagliptin with
Dosage in Renal/Hepatic Impairment SAXagliptin or SITagliptin.
No dose adjustment.
FIXED-COMBINATION(S)
SIDE EFFECTS Glyxambi: linagliptin/empagliflozin
Frequent (16%): Diarrhea (may begin (an antidiabetic): 5 mg/10 mg, 5 mg/25
within first 2 wks of initiation of treat- mg. Jentadueto: linagliptin/metFOR-
ment). Occasional (7%–2%): Abdominal MIN (an antidiabetic): 2.5 mg/500
pain, flatulence, headache, abdominal mg; 2.5 mg/850 mg; 2.5 mg/1,000 mg.
distention. Rare (1% and Less): Gastro- Jentadueto XR: linagliptin/metFOR-
esophageal reflux, vomiting. MIN (extended-release): 2.5 mg/1,000
mg; 5 mg/1,000 mg.
ADVERSE EFFECTS/TOXIC
REACTIONS uCLASSIFICATION
Severe diarrhea was reported in 2% of PHARMACOTHERAPEUTIC: Dipeptidyl
pts. Viral gastroenteritis was noted in 3% peptidase-4 (DDP-4) inhibitor (glip-
of pts. Fecal incontinence, dehydration tin). CLINICAL: Antidiabetic agent.
was reported in 1%. Dose reduced or
suspended secondary to diarrhea, other
GI adverse reaction. USES
Adjunctive treatment to diet and exercise
NURSING CONSIDERATIONS to improve glycemic control in pts with
BASELINE ASSESSMENT type 2 diabetes alone or in combination
with other antidiabetic agents.
Encourage adequate fluid intake. Assess
bowel sounds for peristalsis. Assess for PRECAUTIONS
abdominal disturbances. Contraindications: Hypersensitivity to lin-
INTERVENTION/EVALUATION agliptin, other DD4 inhibitors. Cautions:
For pts with irritable bowel syndrome, Concurrent use of other hypoglycemics.
assess for improvement in symptoms Not recommended for use in type 1

underlined – top prescribed drug


linagliptin 699
diabetes, diabetic ketoacidosis, history of Type 2 Diabetes Mellitus
pancreatitis, HF. PO: ADULTS, ELDERLY: 5 mg once daily.

ACTION Dosage in Renal/Hepatic Impairment


Slows inactivation of incretin hormones No dose adjustment.
by inhibiting DDP-4 enzyme. Therapeu- SIDE EFFECTS
tic Effect: Incretin hormones increase
insulin synthesis/release from pancreatic Occasional (5%): Nasopharyngitis. Rare
beta cells and decrease glucagon secre- (less than 2%): Cough, headache.
tion from pancreatic alpha cells. Lowers ADVERSE EFFECTS/TOXIC
serum glucose levels. REACTIONS
PHARMACOKINETICS Hypoglycemia reported in 7% of pts.
Rapidly absorbed following PO adminis- Concomitant use of hypoglycemic medi-
tration. Peak plasma concentration: 1.5 cation may increase hypoglycemic risk.
hrs. Extensive tissue distribution. Protein Pancreatitis, hypersensitivity reactions
binding: 70%–99%. Minimal metabolism (angioedema, rash, urticaria, pruritus,
(90% excreted as unchanged metabolite). bronchospasm) occur rarely.
Excreted primarily in enterohepatic system NURSING CONSIDERATIONS
(80%), urine (5%). Half-life: 12 hrs. L
BASELINE ASSESSMENT
LIFESPAN CONSIDERATIONS Check blood glucose, hemoglobin A1c
Pregnancy/Lactation: Unknown if dis- level. Assess pt’s understanding of diabe-
tributed in breast milk. Children: Safety tes management, routine glucose moni-
and efficacy not established. Elderly: No toring. Receive full medication history
age-related precautions noted. including herbal products.
INTERACTIONS INTERVENTION/EVALUATION
DRUG: Strong CYP3A4 inducers (e.g., Monitor blood glucose, hemoglobin A1c
carBAMazepine, phenytoin, rifAMPin) level. Assess for hypoglycemia (diaphore-
may decrease concentration/effect. Antidia- sis, tremors, dizziness, anxiety, headache,
betic agents (e.g., insulin, metFORMIN, tachycardia, perioral numbness, hunger,
SAXagliptin, SITagliptin, sulfonyl- diplopia, difficulty concentrating), hyper-
ureas) may increase risk of hypoglycemia. glycemia (polyuria, polyphagia, polydip-
HERBAL: Ginseng, ginger, other herbs sia, nausea, vomiting, fatigue, Kussmaul
with hypoglycemic activity may increase breathing). Screen for glucose-altering
risk of hypoglycemia. St. John’s wort may conditions: fever, increased activity or
decrease concentration/effect. FOOD: None stress, surgical procedures. Dietary con-
known. LAB VALUES: Decreases serum glu- sult for nutritional education.
cose. May increase serum uric acid.
PATIENT/FAMILY TEACHING
AVAILABILITY (Rx) • Diabetes requires lifelong control.
Tablets: 5 mg. • Diet and exercise are principal parts of
treatment; do not skip or delay meals.
ADMINISTRATION/HANDLING • Test blood glucose regularly. • When
PO taking combination drug therapy or when
• May give without regard to food. glucose demands are altered (fever,
­infection, trauma, stress, heavy physical
INDICATIONS/ROUTES/DOSAGE activity), have hypoglycemic treatment
Note: Dose reduction of insulin and/or available (glucagon, oral dextrose).
insulin secretagogues may be needed. • Monitor daily calorie intake.

Canadian trade name Non-Crushable Drug High Alert drug


700 linezolid

PHARMACOKINETICS
linezolid Rapidly, extensively absorbed after PO
administration. Protein binding: 31%.
lin-ez-oh-lid
Metabolized in liver by oxidation. Ex-
(Apo-Linezolid , Zyvox, Zyvoxam
creted in urine. Half-life: 4–5.4 hrs.
)
Do not confuse Zyvox with LIFESPAN CONSIDERATIONS
Zosyn or Zovirax.
Pregnancy/Lactation: Unknown if dis-
uCLASSIFICATION tributed in breast milk. Children: Safety
and efficacy not established. Elderly: No
PHARMACOTHERAPEUTIC: Oxazoli-
age-related precautions noted.
dinone. CLINICAL: Antibiotic.
INTERACTIONS
USES DRUG: Adrenergic medications (sym-
Treatment of susceptible infections due pathomimetics) may increase effects.
to aerobic and facultative, gram-positive SSRIs (e.g., escitalopram, PARox-
microorganisms, including E. faecium etine, sertraline), SNRIs (e.g., DULox-
(vancomycin-resistant strains only), S. etine, venlafaxine) may increase risk of
aureus (including methicillin-resistant serotonin syndrome. Alcohol, carBAM-
L azepine, maprotiline, tapentadol may
strains), S. agalactiae, S. pneumoniae
(including multidrug-resistant strains), increase adverse effects. HERBAL: Supple-
S. pyogenes. Treatment of pneumonia ments containing caffeine, tyrosine, or
(community-acquired and hospital- tryptophan may precipitate hypertensive
acquired), skin, soft tissue infections crisis. FOOD: Excessive amounts of tyra-
(including diabetic foot infections), mine-containing foods, beverages
bacteremia caused by susceptible van- may cause significant hypertension. LAB
VALUES: May decrease Hgb, neutrophils,
comycin-resistant (VRE) organisms.
OFF-LABEL: Treatment of prosthetic joint
platelets, WBC. May increase serum ALT,
infection. Septic arthritis. AST, alkaline phosphatase, amylase, bili-
rubin, BUN, creatinine, LDH, lipase.
PRECAUTIONS
AVAILABILITY (Rx)
Contraindications: Hypersensitivity to
Injection Premix: 2 mg/mL in 100-mL,
linezolid. Concurrent use or within 2
wks of MAOIs. Cautions: History of sei- 300-mL bags. Powder for Oral Suspen-
sion: 100 mg/5 mL. Tablets: 600 mg.
zures, preexisting myelosuppression,
medications that may cause bone mar- ADMINISTRATION/HANDLING
row depression, uncontrolled hyperten-
sion, pheochromocytoma, carcinoid IV
syndrome, untreated hyperthyroidism, Rate of administration • Infuse over
diabetes, chronic infection; concurrent 30–120 min. • Should be administered
use of SSRIs, SNRIs, tricyclic antidepres- without further dilution.
sants, triptans, buPROPion. Storage • Store at room tempera-
ACTION ture. • Protect from light. • Yellow
color does not affect potency.
Binds to bacterial ribosomal RNA sites,
preventing formation of a complex es- PO
sential for bacterial translation. Thera- • Give without regard to food. •
peutic Effect: Bacteriostatic against Use suspension within 21 days after
enterococci, staphylococci; bactericidal ­reconstitution. Gently invert 3–5 times
against streptococci. before administration. • Do not shake.

underlined – top prescribed drug


liraglutide 701

IV INCOMPATIBILITIES ADVERSE EFFECTS/TOXIC


Amphotericin B complex (Abelcet, AmBi- REACTIONS
some, Amphotec), co-trimoxazole (Bac- Thrombocytopenia, myelosuppression
trim), diazePAM (Valium), erythromycin occur rarely. Antibiotic-associated coli-
(Erythrocin), pentamidine (Pentam IV), tis, other superinfections (abdominal
phenytoin (Dilantin). cramps, severe watery diarrhea, fever)
may result from altered bacterial balance
IV COMPATIBILITIES in GI tract.
Calcium gluconate, dexmedetomidine
(Precedex), heparin, magnesium, potas- NURSING CONSIDERATIONS
sium chloride. BASELINE ASSESSMENT
INDICATIONS/ROUTES/DOSAGE Obtain appropriate culture specimens
Vancomycin-Resistant Infections (VRE)
for sensitivity testing prior to therapy.
PO, IV: ADULTS, ELDERLY, CHILDREN
Obtain baseline CBC, chemistries. Ques-
OLDER THAN 11 YRS: 600 mg q12h. CHIL-
tion medical history as listed in Precau-
DREN 11 YRS AND YOUNGER: 10 mg/kg
tions. Receive full medication history and
q8–12h. Maximum: 600 mg/dose. screen for interactions.
INTERVENTION/EVALUATION
Pneumonia, Complicated Skin/Skin L
Structure Infections
Monitor daily pattern of bowel activity,
PO, IV: ADULTS, ELDERLY, CHILDREN
stool consistency. Mild GI effects may
OLDER THAN 11 YRS: 600 mg q12h. CHIL-
be tolerable, but increasing severity may
DREN 11 YRS AND YOUNGER: 10 mg/kg
indicate onset of antibiotic-associated
q8h. Maximum: 600 mg/dose. colitis. Be alert for superinfection: fever,
vomiting, diarrhea, anal/genital pruritus,
Uncomplicated Skin/Skin Structure oral mucosal changes (ulceration, pain,
Infections erythema). Monitor CBC, platelets, Hgb,
PO: ADULTS, ELDERLY: 600 mg
q12h. chemistries.
CHILDREN OLDER THAN 11 YRS: 600 PATIENT/ FAMILY TEACHING
mg q12h. CHILDREN 5–11 YRS: 10
mg/
kg/dose q12h. Maximum: 600 mg/ • Continue therapy for full length of
dose. CHILDREN YOUNGER THAN 5 treatment. • Doses should be evenly
YRS: 10 mg/kg q8h. Maximum: 600
spaced. • May cause GI upset (may
mg/dose. take with food, milk). • Excessive
amounts of tyramine-containing foods
Usual Neonate Dosage (red wine, aged cheese) may cause se-
PO, IV: NEONATES: 10 mg/kg/dose vere reaction (severe headache, neck
q8–12h. stiffness, diaphoresis, palpitations).
• Avoid alcohol. • Report persistent
Dosage in Renal/Hepatic Impairment diarrhea, nausea, vomiting.
No dose adjustment. Administer after HD
on dialysis days.
SIDE EFFECTS liraglutide
Occasional (9%–2%): Diarrhea, nau-
sea, vomiting, insomnia, constipation, leer-a-gloo-tide
rash, dizziness, fever, headache. Rare (Saxenda, Victoza)
(less than 2%): Altered taste, vaginal j BLACK BOX ALERT jCauses
candidiasis, fungal infection, tongue dose-dependent and treatment dura-
discoloration. tion–dependent thyroid C-cell tumors,
including medullary thyroid cancer.

Canadian trade name Non-Crushable Drug High Alert drug


702 liraglutide

FIXED-COMBINATION(S) PHARMACOKINETICS
Xultophy: liraglutide 3.6 mg/mL and Maximum concentration achieved in
insulin degludec 100 units/mL. 8–12 hrs. Protein binding: 98%. Metabo-
lized to large proteins without a specific
uCLASSIFICATION organ as major route of elimination.
PHARMACOTHERAPEUTIC: Antihy- Half-life: 13 hrs.
perglycemic (glucagon-like peptide-1
[GLP-1]) receptor agonist. CLINICAL: LIFESPAN CONSIDERATIONS
Antidiabetic agent. Pregnancy/Lactation: Unknown if dis-
tributed in breast milk. Children: Safety
and efficacy not established. Elderly: No
USES age-related precautions noted.
Saxenda: Adjunct to diet and increased
physical activity for chronic weight man- INTERACTIONS
agement in adults with body mass index DRUG: May increase hypoglycemic
(BMI) of 30 kg/m2 or greater, or 27 kg/ effect of insulin, sulfonylureas.
m2 or greater, with at least one co-morbid HERBAL: None significant. FOOD: None
condition (e.g., hypertension, diabetes, known. LAB VALUES: Decreases glu-
dyslipidemia). Victoza: Adjunct to diet cose serum levels (when used in com-
L and exercise to improve glycemic control bination with insulin secretagogues
in adults and children 10 yrs of age and [e.g., sulfonylureas]).
older with type 2 diabetes. Reduce risk
of major cardiovascular events (e.g., MI, AVAILABILITY (Rx)
stroke) in adults with type 2 diabetes and SQ, Solution (Prefilled Pen):
established cardiovascular (CV) disease. (Victoza): 18 mg/3 mL. (Saxenda): 18
mg/3 mL. Delivers doses of 0.6 mg, 1.2 mg,
PRECAUTIONS 1.8 mg, 2.4 mg, or 3 mg.
Contraindications: Hypersensitivity to
liraglutide. Personal or family history of ADMINISTRATION/HANDLING
medullary thyroid carcinoma (MTC), pts SQ
with multiple endocrine neoplasia syn- • Insert needle subcutaneously into up-
drome type 2 (MEN2). Saxenda: Preg- per arms, outer thigh, or abdomen, and
nancy. Cautions: History of pancreatitis, inject solution. • Do not inject into ar-
cholelithiasis, alcohol abuse, renal/he- eas of active skin disease or injury such
patic impairment. History of angioedema as sunburns, skin rashes, inflammation,
to other GLP-1 receptor agonists. Do not skin infections, or active psoriasis.
use in type 1 diabetes or diabetic keto- • Rotate injection sites.
acidosis. Medications requiring a narrow Storage • Refrigerate prefilled pens.
therapeutic index or requiring rapid GI • Discard if freezing occurs. • Discard
absorption. pen 30 days after initial use.
ACTION INDICATIONS/ROUTES/DOSAGE
Stimulates release of insulin from pancre- Diabetes (Victoza) With or Without CV
atic beta cells, mimics enhancement of Disease
glucose-dependent insulin secretion, de- SQ: ADULTS, ELDERLY, CHILDREN 10 YRS
creases inappropriate glucagon secre- OF AGE AND OLDER: Initial dose: 0.6
tion, slows gastric emptying, decreases mg once daily for at least 1 wk.
food intake. Therapeutic Effect: (Note: This dose is intended to reduce
Improves glycemic control by increasing GI symptoms during initial titration; it is
postmeal insulin secretion, emptying, in- not effective for glycemic control.) After
creasing satiety. 1 wk, increase dose to 1.2 mg. If 1.2-mg
underlined – top prescribed drug
lisdexamfetamine 703
dose does not result in acceptable glyce- activity/stress, surgical procedures).
mic control, dose can be increased to Consider lowering dose of insulin ana-
1.8 mg. logue to reduce risk of hypoglycemia.
Weight Management (Saxenda) PATIENT/FAMILY TEACHING
SQ: ADULTS, ELDERLY: Initially, 0.6 mg • A health care provider will show you
once daily for 1 week. Increase wkly by how to properly prepare and inject your
0.6 mg/day to a target dose of 3 mg once medication. You must demonstrate cor-
daily. Note: Evaluate change in weight rect preparation and injection techniques
16 wks after initiation. Discontinue if less before using medication at home. • Di-
than 4% of baseline weight not achieved. abetes requires lifelong control. • Pre-
scribed diet, exercise are principal parts
Dosage in Renal/Hepatic Impairment of treatment; do not skip/delay meals.
Use caution. • Continue following dietary instruc-
tions, regular exercise program, regular
SIDE EFFECTS testing of blood glucose level. • Serious
Frequent (greater than 13%): Headache, hypoglycemia may occur when used con-
nausea, diarrhea, liraglutide antibody currently with insulin analogue (e.g.,
resistance. Occasional (13%–6%): Diar- sulfonylurea). • Have source of glu-
rhea, vomiting, dizziness, nervousness, cose available to treat symptoms of low L
dyspepsia. Rare (less than 6%): Weak- blood sugar.
ness, decreased appetite.
ADVERSE EFFECTS/TOXIC
REACTIONS lisdexamfetamine
Serious hypoglycemia may occur when
used concurrently with insulin analogue lis-dex-am-fet-a-meen
(e.g., sulfonylurea); consider lowering (Vyvanse)
dose. j BLACK BOX ALERT jPotential
for drug abuse dependency ex-
NURSING CONSIDERATIONS ists. Assess for abuse potential
and monitor for abuse potential/
BASELINE ASSESSMENT dependence.
Check blood glucose concentration be- Do not confuse lisdexamfeta-
fore administration. Discuss pt’s lifestyle mine with dextroamphetamine,
to determine extent of learning, emo- or Vyvanse with Glucovance,
tional needs. Ensure follow-up instruc- Vivactil, or Vytorin.
tion if pt/family does not thoroughly
understand diabetes management or glu- uCLASSIFICATION
cose testing technique. Dose is gradually PHARMACOTHERAPEUTIC: Amphet-
increased to improve GI tolerance. amine (Schedule II). CLINICAL: CNS
INTERVENTION/EVALUATION
stimulant.
Monitor blood glucose level, food intake.
Assess for hypoglycemia (cool wet skin, USES
tremors, dizziness, anxiety, headache, Treatment of attention-deficit/hyperactiv-
tachycardia, numbness in mouth, hunger, ity disorder (ADHD), moderate to severe
diplopia) or hyperglycemia (polyuria, binge eating disorder (BED).
polyphagia, polydipsia, nausea, vomiting,
dim vision, fatigue, deep rapid breath- PRECAUTIONS
ing). Be alert to conditions that alter Hypersensitivity to lis-
Contraindications:
glucose requirements (fever, increased dexamfetamine, amphetamine products.
Canadian trade name Non-Crushable Drug High Alert drug
704 lisdexamfetamine
Concurrent use or within 2 wks of use LAB VALUES: May increase plasma
of MAOI. Cautions: Hyperthyroidism, corticosteroid.
glaucoma, agitated states, cardiovascu-
lar conditions (hypertension, recent MI, AVAILABILITY (Rx)
ventricular arrhythmias), elderly, psy- Capsules:10 mg, 20 mg, 30 mg, 40 mg, 50
chiatric/seizures, preexisting psychosis mg, 60 mg, 70 mg. Tablets, Chewable: 10
or bipolar disorder, Tourette syndrome. mg, 20 mg, 30 mg, 40 mg, 50 mg, 60 mg.
Avoid use in pts with serious structural
cardiac abnormalities, cardiomyopathy, ADMINISTRATION/HANDLING
arrhythmias, CAD. History of alcohol or PO
drug abuse. • May be given in the morning without
regard to food. • Administer capsule
ACTION whole; pt must not chew. • Capsules
Exact mechanism unknown. Enhances may be opened and dissolved in water
action of DOPamine, norepinephrine by and taken immediately. • Chewable
blocking reuptake from synapses, in- tablets: Tablets must be chewed thor-
creasing levels in extraneuronal space. oughly before swallowing.
Therapeutic Effect: Improves atten-
tion span in ADHD. Reduces severity INDICATIONS/ROUTES/DOSAGE
L of BED. ADHD
Note: Assess for cardiac disease and
PHARMACOKINETICS risk of abuse before initiating.
Rapidly absorbed. Converted to dextro- PO: ADULTS, CHILDREN 6 YRS AND
amphetamine. Excreted in urine. Half- OLDER: Initially, 30 mg once daily in
life: Less than 1 hr. the morning. May increase dosage in
increments of 10 or 20 mg/day at wkly
LIFESPAN CONSIDERATIONS intervals until optimal response obtained.
Pregnancy/Lactation: Has poten- Maximum: 70 mg/day.
tial for fetal harm. Distributed in breast
milk. Children: Safety and efficacy not BED
established in pts younger than 6 yrs. PO: ADULTS, ELDERLY: Initially, 30 mg once
Elderly: No age-related precautions daily in morning. May increase by 20 mg/day
noted. at wkly intervals to a target dose of 50–70
mg once daily. Maximum: 70 mg/day.
INTERACTIONS
Dosage in Renal Impairment
DRUG: MAOIs (e.g., phenelzine, CrCl 30 mL/min or greater: Maximum:
selegiline) may increase hypertensive 70 mg/day. CrCl 15–29 mL/min: Maxi-
effect. May decrease sedative effect of mum: 50 mg/day. CrCl less than 15
antihistamines (e.g., diphenhy­ mL/min or end-stage renal disease:
drAMINE). May decrease hypotensive Maximum: 30 mg/day.
effects of antihypertensives (e.g.,
amLODIPine, lisinopril, valsartan). Dosage in Hepatic Impairment
Haloperidol, lithium, urinary acidi- No dose adjustment.
fying agents (ammonium chloride,
sodium acid phosphate) may de- SIDE EFFECTS
crease therapeutic effect. May decrease Frequent (39%): Decreased appetite. Oc-
concentration/effect of PHENobarbital, casional (19%–9%): Insomnia, upper
phenytoin. Tricyclic antidepressants abdominal pain, headache, irritability,
(e.g., amitriptyline, doxepin) may in- vomiting, weight decrease. Rare (6%–
crease stimulatory effects. HERBAL: None 2%): Nausea, dry mouth, dizziness, rash,
significant. FOOD: None known. affect change, fatigue, tic.
underlined – top prescribed drug
lisinopril 705

ADVERSE EFFECTS/TOXIC Do not confuse lisinopril with


REACTIONS fosinopril, or Prinivil with
Abrupt withdrawal following prolonged Plendil, Pravachol, Prevacid,
administration of high dosage may pro- PriLOSEC, Proventil, or Restoril,
duce extreme fatigue (may last for wks). or Zestril with Desyrel, Restoril,
Prolonged administration to children Vistaril, Zetia, or Zostrix.
with ADHD may produce a suppression Do not confuse lisinopril’s
of weight and/or height patterns. May combination form Zestoretic
produce cardiac irregularities, psychotic with PriLOSEC.
syndrome.
FIXED-COMBINATION(S)
NURSING CONSIDERATIONS Prinzide/Zestoretic: lisinopril/
hydro­CHLOROthiazide (a diuretic):
BASELINE ASSESSMENT 10 mg/12.5 mg, 20 mg/12.5 mg, 20
Assess attention span, impulse control, mg/25 mg.
interaction with others. Question history
of cardiomyopathy, glaucoma, hyper- uCLASSIFICATION
tension, hyperthyroidism, psychiatric PHARMACOTHERAPEUTIC: ACE in-
disorder, renal impairment. Receive full hibitor. CLINICAL: Antihypertensive.
medication history and screen for inter- L
actions.
USES
INTERVENTION/EVALUATION
Treatment of hypertension in adults and
Monitor for CNS stimulation, increase in children 6 yrs and older. Adjunctive ther-
B/P, weight loss, pulse, sleep pattern, ap- apy to reduce signs/symptoms of systolic
petite; palpitations, cardiac arrhythmia. HF. Treatment of acute MI within 24 hrs
Observe for signs of hostility, aggression, in hemodynamically stable pts to improve
depression. survival.
PATIENT/FAMILY TEACHING
PRECAUTIONS
• Take early in day. • May mask ex-
treme fatigue. • Report pronounced Contraindications: Hypersensitivity to lisi­
dizziness, decreased appetite, dry mouth, nopril, other ACE inhibitors. History of
weight loss, new or worsened psychiatric angioedema from treatment with ACE inhib-
problems, palpitations, dyspnea. • Sud- itors, idiopathic or hereditary angioedema.
denly stopping treatment may cause Concomitant use with aliskiren in pts with
extreme fatigue that can last for wks. Dis- diabetes. Co-administration with or within
continuance must be done under the 36 hrs of switching to or from a neprilysin
close supervision of health care profes- inhibitor (e.g., sacubitril). Cautions: Renal
sional. impairment, unstented unilateral/bilateral
renal artery stenosis, volume depletion,
ischemic heart disease, cerebrovascular
disease, severe aortic stenosis, hyper-
trophic cardiomyopathy, HF, systolic B/P
lisinopril less than 100, dialysis, hyponatremia; be-
fore, during, or immediately after major
lye-sin-o-pril surgery. Concomitant use of potassium
(Prinivil, Qbrelis, Zestril) supplements.
j BLACK BOX ALERT jMay
cause fetal injury, mortality. Dis- ACTION
continue as soon as possible once
pregnancy is detected. Competitive inhibitor of angiotensin-
converting enzyme (ACE) (prevents

Canadian trade name Non-Crushable Drug High Alert drug


706 lisinopril
conversion of angiotensin I to angio- INDICATIONS/ROUTES/DOSAGE
tensin II, a potent vasoconstrictor; may Hypertension
inhibit angiotensin II at local vascular, PO: ADULTS: Initially, 5–10 mg once
renal sites). Decreases plasma angio- daily. Evaluate response q4–6wks
tensin II, increases plasma renin activity, and titrate dose in 1-step increments
decreases aldosterone secretion. Thera- prn (e.g., increase the daily dose by
peutic Effect: Reduces blood pressure. doubling), up to 40 mg once daily. EL-
DERLY: Initially, 2.5–5 mg once daily.
PHARMACOKINETICS
Evaluate response q4–6wks and titrate
Route Onset Peak Duration dose in 1-step increments prn (e.g., in-
PO 1 hr 6 hrs 24 hrs crease the daily dose by doubling), up
Incompletely absorbed from GI tract. to 40 mg once daily. CHILDREN 6 YRS OR
Protein binding: 25%. Primarily excreted OLDER: Initially, 0.07 mg/kg once daily
unchanged in urine. Removed by hemo- (up to 5 mg). Titrate at 1- to 2-wk in-
dialysis. Half-life: 12 hrs (increased in tervals. Maximum: 0.6 mg/kg/day or
renal impairment). 40 mg/day.

LIFESPAN CONSIDERATIONS HF
Pregnancy/Lactation: Crosses placen­ta. PO: ADULTS, ELDERLY: Initially, 2.5–5
L mg/day. May increase by no more than
Unknown if distributed in breast milk. Chil-
dren: Safety and efficacy not established. 10 mg/day at intervals of at least 2 wks
Elderly: May be more sensitive to hypo- to a target dose of 20–40 mg once daily.
tensive effects. Acute MI (to improve survival)
INTERACTIONS PO: ADULTS, ELDERLY: Initially, 2.5–5
mg, then titrate slowly to 10 mg/day or
DRUG: Aliskiren may increase hyperkale- higher, if tolerated.
mic effect. May increase potential for aller-
gic reactions to allopurinol. Angiotensin Dosage in Renal Impairment
receptor blockers (e.g., losartan, val- CrCl less than 30 mL/min: Not recom-
sartan) may increase adverse effects. mended in children. Titrate to pt’s needs
May increase adverse effects of lithium, after giving the following initial dose:
sacubitril. HERBAL: Herbals with hy-
pertensive properties (e.g., licorice, Hypertension
yohimbe) or hypotensive properties Creatinine Clearance Initial Dose
(e.g., garlic, ginger, ginkgo biloba) 10–30 mL/min 5 mg
may alter effects. FOOD: None known. Less than 10 mL/min or 2.5 mg
LAB VALUES: May increase serum BUN, ­Dialysis
alkaline phosphatase, bilirubin, creatinine,
potassium, ALT, AST. May decrease serum HF
sodium. May cause positive ANA titer. CrCl less than 30 mL/min or serum
creatinine greater than 3 mg/dL:
AVAILABILITY (Rx)
Initial dose: 2.5 mg.
Solution, Oral: (Qbrelis): 1 mg/mL. Tab-
lets: 2.5 mg, 5 mg, 10 mg, 20 mg, 30 Acute MI
mg, 40 mg. CrCl 30 mL/min or less: Initial dose:
2.5 mg.
ADMINISTRATION/HANDLING
PO Dosage in Hepatic Impairment
• Give without regard to food. • Tab- No dose adjustment.
lets may be crushed.

underlined – top prescribed drug


lithium 707

SIDE EFFECTS place pt in supine position, feet slightly


Frequent (12%–5%): Headache, dizzi- elevated.
ness, postural hypotension. Occasional PATIENT/ FAMILY TEACHING
(4%–2%): Chest discomfort, fatigue,
• To reduce hypotensive effect, go from
rash, abdominal pain, nausea, diarrhea,
lying to standing slowly. • Limit alcohol
upper respiratory infection. Rare (1% or
intake. • Report vomiting, diarrhea,
less): Palpitations, tachycardia, periph-
diaphoresis, swelling of face/lips/tongue,
eral edema, insomnia, paresthesia, con-
difficulty in breathing, persistent cough.
fusion, constipation, dry mouth, muscle
• Limit salt intake. • Maintain ade-
cramps.
quate hydration. • Report decreased
ADVERSE EFFECTS/TOXIC urinary output, dark-colored urine,
REACTIONS swelling of the hands and feet. • Im-
mediately report allergic reactions, esp.
Excessive hypotension (first-dose syn-
life-threatening swelling of the face or
cope) may occur in pts with HF, severe
tongue.
salt/volume depletion. Angioedema
(swelling of face and lips), hyperkalemia
occur rarely. Agranulocytosis, neutro-
penia may be noted in pts with collagen
vascular disease (scleroderma, systemic
lithium L
lupus erythematosus). Nephrotic syn- lith-ee-um
drome may be noted in pts with history (Carbolith , Lithobid, Lithane ,
of renal disease. Lithmax )
NURSING CONSIDERATIONS j BLACK BOX ALERT j Lithium
toxicity is closely related to serum
BASELINE ASSESSMENT lithium levels and can ­occur at thera-
peutic doses. ­Routine ­determination
Obtain BMP (esp. serum BUN, creatinine, of serum lithium levels is essential
sodium, potassium; CrCl, GFR. Obtain B/P, during therapy.
apical pulse immediately before each dose Do not confuse Lithobid with
in addition to regular monitoring (be alert Levbid or Lithostat.
to fluctuations). In pts with renal impair-
ment, autoimmune disease, taking drugs uCLASSIFICATION
that affect leukocytes or immune response, PHARMACOTHERAPEUTIC: Mood-
CBC and differential count should be per- stabilizing agent. CLINICAL: Anti-
formed before beginning therapy and manic.
q2wks for 3 mos, then periodically there-
after. Question history of aortic stenosis,
cardiac disease, cardiomyopathy, renal USES
impairment or stenosis. Management of bipolar disorder. Treat-
INTERVENTION/EVALUATION ment of mania in pts with bipolar dis-
order. OFF-LABEL: Augmenting agent for
Monitor B/P, renal function tests, WBC,
depression.
serum potassium. Assess for edema.
Auscultate lungs for rales. Monitor PRECAUTIONS
I&O; weigh daily. Monitor daily pattern
Contraindications: Hypersensitivity to
of bowel activity, stool consistency. As-
lith­ium. Severely debilitated pts, severe
sist with ambulation if dizziness occurs.
cardiovascular disease, concurrent use
If excessive reduction in B/P occurs,
with diuretics, severe dehydration, severe

Canadian trade name Non-Crushable Drug High Alert drug


708 lithium
renal disease, severe sodium depletion or adverse effects. HERBAL: None sig-
dehydration. Cautions: Mild to moderate nificant. FOOD: None known. LAB
cardiovascular disease, thyroid disease, VALUES: May increase serum glucose,
elderly, mild to moderate renal impair- immunoreactive parathyroid hormone,
ment, medications altering sodium ex- calcium. Therapeutic serum level:
cretion, pregnancy, pts at risk for suicide, 0.6–1.2 mEq/L; toxic serum level:
pts with significant fluid loss, pts receiv- greater than 1.5 mEq/L.
ing neuromuscular blocking agents.
AVAILABILITY (Rx)
ACTION Capsules: 150 mg, 300 mg, 600 mg.
Exact mechanism unknown. Alters cation Oral Solution: 8 mEq/5 mL (equivalent
transport across cell membrane in nerve/ to 300 mg lithium carbonate). Tablets:
muscle cells; influences reuptake of sero- 300 mg.
tonin/norepinephrine. Therapeutic Ef- Tablets (Extended-Release): 300 mg,
fect: Stabilizes mood, reducing episodes 450 mg.
of mania.
ADMINISTRATION/HANDLING
PHARMACOKINETICS
PO
Rapidly, completely absorbed from GI • Administer with meals, milk to decrease
L tract. Protein binding: None. Primarily GI upset. • Do not break, crush, dis-
excreted unchanged in urine. Removed solve, or divide extended-release t­ablets.
by hemodialysis. Half-life: 18–24 hrs
(increased in elderly). INDICATIONS/ROUTES/DOSAGE
LIFESPAN CONSIDERATIONS b ALERT c During acute phase, a thera-
Pregnancy/Lactation: Freely crosses peutic serum lithium concentration of
placenta. Distributed in breast milk. 0.6–1.2 mEq/L is required. For long-term
Children: May increase bone formation
control, desired level is 0.8–1 mEq/L.
or density (alter parathyroid hormone Monitor serum drug concentration, clini-
concentrations). Elderly: More suscep- cal response to determine proper dosage.
tible to develop lithium-induced goiter Usual Dosage
or clinical hypothyroidism, CNS toxicity. PO: ADULTS, ELDERLY, CHILDREN OLDER
Increased thirst, urination noted more THAN 12 YRS: (Immediate-Release):
frequently; lower dosage recommended. 300 mg 3–4 times/day. Gradually increase
INTERACTIONS (e.g., 300–600 mg q1–5 days) based on
response/tolerability. Usual dose: (Imme-
DRUG: Diuretics (e.g., furosemide, diate-Release): 900–1,800 mg/day in
hydroCHLOROthiazide), NSAIDs 1–3 divided doses. (Extended-Release):
(e.g., ibuprofen, naproxen, ke- 450 mg twice daily. Gradually increase
torolac), metroNIDAZOLE, ACE in- based on response/tolerability. Usual
hibitors (e.g., enalapril, lisinopril), dose: (Extended-Release): 900–1,800
angiotensin II antagonists (e.g., mg in 2 divided doses.
losartan, valsartan), SSRIs (e.g., es-
citalopram, PARoxetine, sertraline), Dosage in Renal Impairment
calcium channel blockers (e.g., am- Creatinine Clearance Dosage
LODIPine, dilTIAZem, verapamil)
10–50 mL/min 50%–75%
may increase lithium concentration, normal dose
risk of toxicity. May increase neurotoxic Less than 10 mL/min 25%–50%
effect of tricyclic antidepressants normal dose
(e.g., amitriptyline). MAOIs (e.g., End-stage renal disease Dose after HD
phenelyzine, selegiline) may increase with HD

underlined – top prescribed drug


lixisenatide 709
Dosage in Hepatic Impairment Assess for increased urinary output,
No dose adjustment. ­persistent thirst. Report polyuria, pro-
longed vomiting, diarrhea, fever to physi-
SIDE EFFECTS cian (may need to temporarily reduce or
b ALERT c Side effects are dose related discontinue dosage). Monitor for signs
and seldom occur at lithium serum levels of lithium toxicity. Assess for therapeutic
less than 1.5 mEq/L. Occasional: Fine response (interest in surroundings, im-
hand tremor, polydipsia, polyuria, mild provement in self-care, increased ability
nausea. Rare: Weight gain, bradycardia, to concentrate, relaxed facial expres-
tachycardia, acne, rash, muscle twitch- sion). Monitor lithium levels q3–4days
ing, peripheral cyanosis, pseudotumor at initiation of therapy (then q1–2mos).
cerebri (eye pain, headache, tinnitus, vi- Obtain lithium levels 8–12 hrs postdose.
sion disturbances). Therapeutic serum level: 0.6–1.2
mEq/L; toxic serum level: greater than
ADVERSE EFFECTS/TOXIC 1.5 mEq/L.
REACTIONS
Lithium serum concentration of 1.5–2.0 PATIENT/ FAMILY TEACHING
mEq/L may produce vomiting, diarrhea, • Limit alcohol, caffeine intake. • Avoid
drowsiness, confusion, incoordination, tasks requiring coordination until CNS
coarse hand tremor, muscle twitching, effects of drug are known. • May cause L
T-wave depression on ECG. Lithium se- dry mouth. • Maintain adequate salt,
rum concentration of 2.0–2.5 mEq/L fluid intake (avoid dehydration). • Re-
may result in ataxia, giddiness, tinnitus, port vomiting, diarrhea, muscle weak-
blurred vision, clonic movements, severe ness, tremors, drowsiness, ataxia.
hypotension. Acute toxicity may be char- • Monitoring of serum level is necessary
acterized by seizures, oliguria, circula- to determine proper dose.
tory failure, coma, death.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
lixisenatide
Question history of cardiac/thyroid dis- lix-i-sen-a-tide
ease, renal impairment. Assess hydration (Adlyxin)
status. Assess mental status (e.g., mood, Do not confuse lixisenatide with
behavior). Serum lithium levels should exenatide, liraglutide.
be tested q3–4days during initial phase
of therapy, q1–2mos thereafter, and wkly FIXED-COMBINATION(S)
if there is no improvement of disorder or Soliqua: lixisenatide 33 mcg/mL and
adverse effects occur. insulin glargine 100 units/mL.
INTERVENTION/EVALUATION
uCLASSIFICATION
Clinical assessment of therapeutic effect,
tolerance to drug effect is necessary for PHARMACOTHERAPEUTIC: Antihy-
correct dosing-level management. As- perglycemic (glucagon-like peptide-1
sess behavior, appearance, emotional [GLP-1]) receptor agonist. CLINICAL:
status, response to environment, speech Antidiabetic agent.
pattern, thought content. Monitor serum
lithium concentrations, CBC with differ- USES
ential, urinalysis, creatinine clearance.
Adjunct to diet and exercise to improve
Monitor renal, hepatic, thyroid, cardio-
glycemic controls in pts with type 2 dia-
vascular function; serum electrolytes.
betes mellitus.

Canadian trade name Non-Crushable Drug High Alert drug


710 lixisenatide

PRECAUTIONS guidelines. • Visually inspect for par-


Contraindications: Hypersensitivity to ticulate matter or discoloration. Solution
lixisenatide. Cautions: Renal impair- should appear clear and color-
ment, severe gastroparesis, history of less. • Do not use if solution is cloudy
pancreatitis. Not recommended in pts or discolored or if visible particles are
with diabetic ketoacidosis, type 1 diabe- observed.
tes mellitus. Not a substitute for insulin. Administration • Administer within 1
Medications with narrow therapeutic hr before the first meal of the day, prefer-
index or requiring rapid GI absorption. ably the same time each day. If a dose is
missed, administer within 1 hr prior to
ACTION next meal. • Insert needle subcutane-
Increases glucose-dependent insulin ously into upper arms, outer thigh, or
secretion; decreases inappropriate glu- abdomen, and inject solution. • Do not
cagon secretion. Slows gastric emptying. inject into areas of active skin disease
Therapeutic Effect: Improves glyce- or injury such as sunburns, skin rashes,
mic control by lowering fasting glucose inflammation, skin infections, or active
and postprandial blood glucose. psoriasis. • Rotate injection sites.
Storage • Refrigerate unused injector
PHARMACOKINETICS pens. • Once injector pen is activated,
L store at room temperature for up to 14
Widely distributed. Protein binding: not
days. • Do not freeze. • Protect from
specified. Peak plasma concentration:
light.
1–3.5 hrs. Eliminated through glomeru-
lus filtration and proteolytic degradation. INDICATIONS/ROUTES/DOSAGE
Half-life: 3 hrs. Type 2 Diabetes Mellitus
SQ: ADULTS, ELDERLY: 10 mcg once
LIFESPAN CONSIDERATIONS daily for 14 days. Increase to 20 mcg
Pregnancy/Lactation: Unknown if once daily on day 15. Maintenance: 20
distributed in breast milk. Children: mcg once daily.
Safety and efficacy not established. El-
derly: No age-related precautions Dosage in Renal Impairment
noted. Use caution.

INTERACTIONS Dosage in Hepatic Impairment


No dose adjustment.
DRUG: May increase hypoglycemic effect
when added to insulin or sulfonylureas. SIDE EFFECTS
May decrease concentration/effect of oral
Frequent (25%–10%): Nausea, vomiting.
contraceptives. Oral contraceptive
Occasional (9%–1%): Headache, diarrhea,
should be taken 1 hr before or 11 hrs af-
dizziness, dyspepsia, constipation, ab-
ter lixisenatide. HERBAL: None significant.
dominal distention, abdominal pain.
FOOD: None known. LAB VALUES: Ex-
pected to decrease serum glucose, Hgb A1c. ADVERSE EFFECTS/TOXIC
REACTIONS
AVAILABILITY (Rx)
May increase risk of acute renal failure
Prefilled Injector Pens: 10 mcg/0.2 mL,
or worsening of chronic renal impair-
20 mcg/0.2 mL.
ment (esp. in pts with vomiting, dehydra-
ADMINISTRATION/HANDLING tion). May increase risk of hypoglycemia
when used with other hypoglycemic
SQ agents or insulin. Anaphylaxis reported
Preparation • Follow instructions for in less than 1% of pts. Other hypersen-
preparation according to manufacturer sitivity reactions including angioedema,
underlined – top prescribed drug
lomitapide 711
bronchospasm, laryngeal edema occur rash, swelling of the face or throat.
rarely. Acute pancreatitis, hemorrhagic • Oral contraceptives should be taken at
or necrotizing pancreatitis were re- least 1 hr before or 11 hrs after dose.
ported. Immunogenicity (auto-lixisena- • Therapy may cause acute kidney in-
tide antibodies) occurred in 70% of pts. jury or kidney failure; report decreased
urine output, amber-colored urine,
NURSING CONSIDERATIONS flank pain.
BASELINE ASSESSMENT
Obtain baseline fasting glucose level,
Hgb A1c; BMP. Question history of renal
impairment, gastroparesis, hypersen-
lomitapide
sitivity reaction. Screen for use of other lom-i-ta-pide
hypoglycemic agents or insulin. Assess (Juxtapid)
pt’s understanding of diabetes manage-
ment, routine home glucose monitoring, j BLACK BOX ALERT jMay
cause hepatotoxicity. May cause
medication self-administration. Assess hepatic steatosis (increase in
hydration status. Obtain dietary consult hepatic fat) regardless of serum
for nutritional education. ALT, AST elevation; may be risk
factor for progressive hepatic
INTERVENTION/EVALUATION disease, including steatohepatitis L
Monitor capillary blood glucose levels, Hgb and cirrhosis.
A1c; renal function test (esp. in pts with Do not confuse lomitapide with
renal impairment who report diarrhea, loperamide.
gastroparesis, vomiting). Assess for hypo- uCLASSIFICATION
glycemia (anxiety, confusion, diaphoresis,
diplopia, dizziness, headache, hunger, PHARMACOTHERAPEUTIC: Micro-
perioral numbness, tachycardia, trem- somal triglyceride transfer protein
ors), hyperglycemia (confusion, fatigue, (MTP) inhibitor. CLINICAL: Antihy-
Kussmaul breathing, nausea, polyuria, perlipidemic.
vomiting). Screen for glucose-altering con-
ditions: fever, stress, surgical procedures,
trauma. Monitor for hypersensitivity reac- USES
tions; abdominal pain that radiates to the Treatment of homozygous familial hyper-
back. Encourage fluid intake. Monitor I&O. cholesterolemia (HoFH) in combination
with low-fat diet and other lipid-lowering
PATIENT/FAMILY TEACHING therapies, including LDL-C apheresis, to
• Diabetes requires lifelong control. reduce LDL, total cholesterol, apoprotein
Diet and exercise are principal parts of B, non–HDL-C.
treatment; do not skip or delay meals.
• Test blood sugar regularly. • Moni- PRECAUTIONS
tor daily calorie intake. • When taking Contraindications:Hypersensitivity to
additional medications to lower blood lomitapide. Pregnancy, breastfeeding,
sugar or when glucose demands are al- moderate to severe hepatic impair-
tered (fever, infection, stress trauma), ment, active hepatic disease includ-
have low blood sugar treatment available ing unexplained persistent elevation
(glucagon, oral dextrose). of serum transaminases, concomitant
• Persistent, severe abdominal pain that use of strong CYP3A4 inhibitors. Cau-
radiates to the back (with or without tions: Mild to moderate renal impair-
vomiting) may indicate acute pancreati- ment, end-stage renal disease, mild
tis. • Report allergic reactions of any hepatic impairment, alcohol consump-
kind, esp. difficulty breathing, itching, tion. Avoid use in pts with history of
Canadian trade name Non-Crushable Drug High Alert drug
712 lomitapide
glucose-galactose malabsorption, other AVAILABILITY (Rx)
agents having hepatotoxic potential
Capsules: 5 mg, 10 mg, 20 mg, 30
(e.g., acetaminophen).
mg, 40 mg, 60 mg.
ACTION ADMINISTRATION/HANDLING
Inhibits microsomal triglyceride trans- PO
fer protein (MTP) in lumen of endo- • Give with water only. • Adminis-
plasmic reticulum. Prevents assembly ter without food (at least 2 hrs after
of apo-B-containing lipoproteins in evening meal). • Administer whole;
enterocytes, hepatocytes; inhibits syn- do not break, crush, or open cap-
thesis of chylomicrons, very low density sules.
lipoprotein (VLDL). Therapeutic Ef-
fect: Decreases plasma low-density li- INDICATIONS/ROUTES/DOSAGE
poprotein cholesterol (LDL-C). b ALERT c To reduce risk for fat-
soluble nutrient deficiency, recom-
PHARMACOKINETICS mend supplemental coadministration:
Well absorbed in GI tract. Metabolized in vitamin E 400 international units PO
liver. Protein binding: 99%. Peak plasma daily, linolenic acid 200 mg PO daily,
concentration: 6 hrs. Primarily excreted alpha-linolenic acid (ALA) 210 mg PO
L in feces. Half-life: 40 hrs. daily, eicosapentaenoic acid (EPA)
110 mg PO daily, docosahexaenoic
LIFESPAN CONSIDERATIONS acid (DHA) 80 mg PO daily. Because
Pregnancy/Lactation: Contraindicated of risk for myopathy, concurrent use
in pregnancy. May cause fetal harm. Must of simvastatin should not exceed 20–
use effective contraception in addition to 40 mg/day.
barrier methods. Unknown if distributed
in breast milk. Must either discontinue Homozygous Familial
breastfeeding or discontinue therapy. Hypercholesterolemia (HoFH)
Children: Safety and efficacy not estab- PO: ADULTS, ELDERLY: Initially, 5 mg
lished. Elderly: Increased risk for side once daily for minimum of 2 wks. Then,
effects, adverse reactions. may increase dose to 10 mg once daily,
then may increase dose at 4-wk (mini-
INTERACTIONS mum) intervals to 20 mg once daily, then
DRUG: Acetaminophen may in- 40 mg once daily, then 60 mg once daily
crease risk for hepatotoxicity. Strong based on tolerability. Maximum: 60
CYP3A4 inhibitors (e.g., clarithro- mg/day.
mycin, ketoconazole, ritonavir) Dose Modification
contraindicated due to increased risk Elevated Hepatic Enzymes
for myopathy, rhabdomyolysis. Mod- If ALT, AST is between 3–5 times upper
erate CYP3A4 inhibitors (e.g., limit of normal (ULN), reduce dose until
atorvastatin, oral contraceptives) ALT, AST less than 3 times ULN. If ALT,
may increase concentration. May in- AST is greater than 5 times ULN, with-
crease concentration of warfarin. hold dose until less than 3 times ULN,
Ciprofloxacin may increase con- then restart at reduced dose. If hepa-
centration/effect. HERBAL: St. John’s totoxicity occurs or bilirubin level rises
wort may decrease concentration/ greater than 2 times ULN, discontinue
effect. FOOD: Grapefruit products treatment.
may increase absorption, toxicity. LAB End-Stage Renal Disease Receiving
VALUES: May increase serum alkaline
Dialysis, Mild Hepatic Impairment
phosphatase, bilirubin, ALT, AST. Do not exceed 40 mg/day.

underlined – top prescribed drug


loperamide 713
Concurrent Use of Weak CYP3A4 ­ btain baseline laboratory studies: ALT,
O
Inhibitors AST, alkaline phosphatase, bilirubin, se-
Do not exceed 30 mg/day. rum cholesterol, triglycerides, PT/INR (if
Concurrent Use of Oral Contraception pt is on warfarin). Confirm positive his-
Do not exceed 40 mg/day. tory of homozygous familial hypercholes-
terolemia (HoFH). Receive full medica-
Dosage in Renal Impairment tion history including vitamins, minerals,
No dose adjustment. End-stage renal herbal products. Screen for medical his-
disease: Maximum: 40 mg/day. tory as listed in Precautions.
Dosage in Hepatic Impairment INTERVENTION/EVALUATION
Mild impairment: Maximum: 40 mg/ Maintain hydration; offer fluids fre-
day. Moderate to severe impairment: quently. Monitor INR routinely (with
Contra­indi­cated. anticoagulants). Monitor LFT with any
SIDE EFFECTS dosage change, then every month for first
year when maintenance goal reached,
Frequent (79%–65%): Diarrhea, nau- then every 3 mos. Obtain ECG for palpi-
sea. Occasional (38%–10%): Dyspepsia, tations, shortness of breath, dizziness.
vomiting, abdominal pain, weight loss, Monitor for bruising, hematuria, jaun-
abdominal distention, constipation, flatu- dice, right upper abdominal pain, fever, L
lence, fatigue, back pain, gastric reflux, lethargy, melena.
headache, dizziness.
PATIENT/FAMILY TEACHING
ADVERSE EFFECTS/TOXIC • Avoid pregnancy. • Use appropriate
REACTIONS contraception measures, including barrier
Progressive hepatic disease including precautions. • If pregnancy occurs, in-
steatohepatitis, cirrhosis has been re- form physician immediately. • Diarrhea
ported in 6% of pts due to increased may decrease effectiveness of oral contra-
hepatic fat. May reduce absorption of ception. • Do not breastfeed. • Main-
fat-soluble nutrients; recommend daily tain low-fat diet. • Report yellowing of
supplemental replacement. Increased skin, bruising, black/tarry stool, right up-
risk for myopathy including rhabdomy- per quadrant pain, fever, lethargy, chest
olysis (muscle pain/tenderness, weak- pain, palpitations. • Avoid alco-
ness, dark or decreased urine output, hol. • Avoid grapefruit products. • Do
elevated serum creatinine, CPK) when not chew, crush, or open capsules. • Re-
used with other antihyperlipidemics. port any newly prescribed medications.
May increase risk for supratherapeutic
INR with warfarin. Infections including
influenza, nasopharyngitis, gastroenteri-
tis reported in 5% of pts. Palpitations,
loperamide
angina pectoris reported in 3% of pts. loe-per-a-myde
Increased risk for dehydration/mal- (Diamode, Diarr-Eze , Imodium
absorption with galactose intolerance A-D, Loperacap )
hereditary disorder, pancreatic disease, Do not confuse Imodium with
diarrhea. Indocin, or loperamide with
NURSING CONSIDERATIONS furosemide.
BASELINE ASSESSMENT FIXED-COMBINATION(S)
Obtain detailed dietary history, esp. fat Imodium Advanced: loperamide/
consumption. Confirm negative preg- simethicone (an antiflatulent): 2
nancy test before initiating treatment. mg/125 mg.

Canadian trade name Non-Crushable Drug High Alert drug


714 loperamide
uCLASSIFICATION LIFESPAN CONSIDERATIONS
PHARMACOTHERAPEUTIC: Antidiar- Pregnancy/Lactation: Unknown if
rheal agent. CLINICAL: Antidiarrheal. drug crosses placenta or is distributed
in breast milk. Children: Not recom-
mended for pts younger than 2 yrs
USES (infants younger than 3 mos more sus-
Controls, provides symptomatic re- ceptible to CNS effects). Elderly: May
lief of acute nonspecific diarrhea in mask dehydration, electrolyte depletion.
pts 2 yrs and older, chronic diarrhea
associated with inflammatory bowel INTERACTIONS
disease; reduces volume of ileostomy DRUG: May increase concentration/ef-
discharge. OTC: Control symptoms of fects of QT-prolonging agents (e.g.,
diarrhea, including traveler’s diarrhea. amiodarone, haloperidol, so-
OFF-LABEL: Chemotherapy-induced talol). Ranolazine may increase lev-
diarrhea, irinotecan-induced delayed els/effects. HERBAL: None significant.
diarrhea. FOOD: None known. LAB VALUES: None
significant.
PRECAUTIONS
Contraindications: Hypersensitivity to AVAILABILITY (Rx)
L loperamide. Abdominal pain without Capsules: 2 mg. Liquid: 1 mg/5 mL, 1
diarrhea; children younger than 2 yrs; mg/7.5 mL. Suspension, Oral: 1 mg/7.5
acute dysentery, acute ulcerative coli- mL. Tablet: 2 mg.
tis, bacterial enterocolitis caused by
invasive organisms, including Salmo- ADMINISTRATION/HANDLING
nella, Shigella, Campylobacter; pseu- Liquid
domembranous colitis associated • When administering to children, use
with broad-spectrum antibiotic use. accompanying plastic dropper to mea-
Cautions: Hepatic impairment, use in sure the liquid.
young children. Avoid use when inhibi- INDICATIONS/ROUTES/DOSAGE
tion of peristalsis is undesirable (e.g.,
potential for ileus, megacolon). Avoid Acute Diarrhea
use in pts with risk factors for QT PO: (Capsules): ADULTS, ELDERLY: Ini-
prolongation. tially, 4 mg, then 2 mg after each un-
formed stool. Maximum: 16 mg/day.
ACTION CHILDREN 9–12 YRS, WEIGHING MORE THAN
30 KG: Initially, 2 mg 3 times/day for 24
Directly affects intestinal wall muscles
through opioid receptor. Therapeutic hrs, then 0.1 mg/kg/dose after each loose
Effect: Slows intestinal motility, pro- stool. Maximum: 6 mg/day. CHILDREN
6–8 YRS, WEIGHING 20–30 KG: Initially, 2
longs transit time of intestinal contents by
reducing fecal volume, diminishing loss mg twice daily for 24 hrs, then 0.1 mg/kg/
of fluid, electrolytes, increasing viscos- dose after each loose stool. Maximum: 4
ity, bulk of stool. Increases tone of anal mg/day. CHILDREN 2–5 YRS, WEIGHING 13–20
KG: Initially, 1 mg 3 times/day for 24 hrs,
sphincter.
then 0.1 mg/kg/dose after each loose
PHARMACOKINETICS stool. Maximum: 3 mg/day.
Poorly absorbed from GI tract. Protein Chronic Diarrhea
binding: 97%. Metabolized in liver. Ex- PO: ADULTS, ELDERLY: Initially, 4 mg, then
creted in feces (30%), urine (less than 2 mg after each unformed stool until diar-
2%). Not removed by hemodialysis. rhea is controlled. Average maintenance
Half-life: 9–14 hrs. dose: 4–8 mg/day. Maximum: 16 mg/day.

underlined – top prescribed drug


loratadine 715
Traveler’s Diarrhea is established. • Report diarrhea last-
PO: ADULTS, ELDERLY: Initially, 4 ing more than 3 days, abdominal pain
mg, then 2 mg after each loose bowel with distention, new-onset fever.
movement (LBM). Maximum: 16 mg/
day (OTC: 8 mg/day). CHILDREN 9–11
YRS: Initially, 2 mg, then 1 mg after each loratadine
LBM. Maximum: 6 mg/day. CHILDREN
6–8 YRS: Initially, 2 mg, then 1 mg after lor-at-a-deen
each LBM. Maximum: 4 mg/day. (Alavert, Apo-Loratadine , Claritin,
Dosage in Renal/Hepatic Impairment
Claritin Reditabs, Loradamed)
No dose adjustment. Do not confuse loratadine
with clonidine, or Claritin with
SIDE EFFECTS clarithromycin.
Rare: Dry mouth, drowsiness, abdomi- FIXED-COMBINATION(S)
nal discomfort, allergic reaction (rash,
pruritus). Alavert Allergy and Sinus, Clari-
tin-D: loratadine/pseudoephedrine (a
ADVERSE EFFECTS/TOXIC sympathomimetic): 5 mg/120 mg, 10
REACTIONS mg/240 mg.
L
Toxicity results in constipation, GI irrita- uCLASSIFICATION
tion (nausea, vomiting), CNS depression.
PHARMACOTHERAPEUTIC: H1 antago-
Activated charcoal is used to treat loper-
amide toxicity. nist, second generation. CLINICAL: An-
tihistamine.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT USES
Do not administer if GI bleeding, me- Relief of nasal, non-nasal symptoms of sea-
chanical obstruction is suspected. Inves- sonal allergic rhinitis (hay fever). Treat-
tigate cause of diarrhea (infectious vs. ment of itching due to hives (urticaria).
noninfectious). The use of antidiarrheals
in the presence of C. difficile–associated PRECAUTIONS
diarrhea or other diarrhea caused by bac- Contraindications: Hypersensitivity to lo-
teria is controversial (drug may inhibit ratadine. Cautions: Renal/hepatic impair­
expulsion of toxic bacteria while elderly ment.
and debilitated pts are at an increased risk
of mortality due to dehydration). ACTION
Competes with histamine for H1 receptor
INTERVENTION/EVALUATION
sites on effector cells. Therapeutic Ef-
Encourage adequate fluid intake. Assess fect: Prevents allergic responses medi-
bowel sounds for peristalsis. Monitor ated by histamine (e.g., rhinitis, urticaria,
daily pattern of bowel activity, stool con- pruritus).
sistency. Withhold drug, notify physician
promptly in event of abdominal pain, dis- PHARMACOKINETICS
tention, fever. Route Onset Peak Duration
PATIENT/FAMILY TEACHING PO 1–3 hrs 8–12 hrs Longer than
24 hrs
• Do not exceed prescribed dose.
• May cause dry mouth. • Avoid alco- Rapidly, almost completely absorbed
hol. • Avoid tasks that require alert- from GI tract. Protein binding: 97%; me-
ness, motor skills until response to drug tabolite, 73%–77%. Distributed mainly to

Canadian trade name Non-Crushable Drug High Alert drug


716 LORazepam
liver, lungs, GI tract, bile. Metabolized in Dosage in Renal Impairment
liver. Excreted in urine (40%) and feces (CrCl less than 30 mL/min)
(40%). Not removed by hemodialysis. PO: ADULTS, ELDERLY, CHILDREN 6 YRS
Half-life: 8.4 hrs; metabolite, 28 hrs (in- AND OLDER: 10 mg every other day. CHIL-
creased in elderly, hepatic impairment). DREN 2–5 YRS: No dose adjustment.

LIFESPAN CONSIDERATIONS Dosage in Hepatic Impairment


Pregnancy/Lactation: Distributed in No dose adjustment.
breast milk. Children: Safety and efficacy
not established in pts younger than 2 yrs. SIDE EFFECTS
Elderly: More sensitive to anticholiner- Frequent (12%–8%): Headache, fatigue,
gic effects (e.g., dry mouth, nose, throat). drowsiness. Occasional (3%): Dry mouth,
nose, throat. Rare: Photosensitivity.
INTERACTIONS
DRUG: Aclidinium, ipratropium, tiotro- ADVERSE EFFECTS/TOXIC
pium, umeclidinium may increase anti- REACTIONS
cholinergic effect. HERBAL: Herbals with None significant.
sedative properties (e.g., chamomile,
kava kava, valerian) may increase CNS de- NURSING CONSIDERATIONS
L pression. FOOD: All foods delay absorption. BASELINE ASSESSMENT
LAB VALUES: May suppress wheal, flare re-
actions to antigen skin testing unless drug is Assess lung sounds for wheezing, skin for
discontinued 4 days before testing. urticaria, other allergy symptoms.
INTERVENTION/EVALUATION
AVAILABILITY (Rx)
For upper respiratory allergies, increase
Capsule: 10 mg. Solution, Oral: 5 mg/5 mL. fluids to decrease viscosity of secretions,
Syrup: 5 mg/5 mL. Tablets: 10 mg. Tab- offset thirst, replenish loss of fluids from
lets, Chewable: 5 mg. Tablets, Orally Dis- increased diaphoresis. Monitor symp-
integrating: 5 mg, 10 mg. toms for therapeutic response.
ADMINISTRATION/HANDLING PATIENT/FAMILY TEACHING
PO • Drink plenty of water (may cause dry
• May take without regard for food. mouth). • Avoid alcohol. • Avoid
tasks that require alertness, motor skills
Orally Disintegrating Tablets until response to drug is established
• Place under tongue. • Disintegra- (may cause drowsiness). • May cause
tion occurs within seconds, after which photosensitivity reactions (avoid direct
tablet contents may be swallowed with or exposure to sunlight).
without water.

INDICATIONS/ROUTES/
DOSAGE LORazepam
Allergic Rhinitis
PO: ADULTS, ELDERLY, CHILDREN 6 YRS AND lor-az-e-pam
OLDER: (Claritin Reditabs): 10 mg once (Ativan, LORazepam Intensol)
daily or 5 mg twice daily. CHILDREN 2–5 Do not confuse Ativan with
YRS: 5 mg once daily. Ambien or Atarax, or LO-
Razepam with ALPRAZolam,
Urticaria diazePAM, Lovaza, temazepam,
PO: ADULTS, ELDERLY: Initially, 10 mg once or zolpidem.
daily. May increase to 10 mg twice daily.

underlined – top prescribed drug


LORazepam 717
uCLASSIFICATION Well absorbed after PO, IM administra-
PHARMACOTHERAPEUTIC: Ben- tion. Protein binding: 85%. Widely dis-
zodiazepine (Schedule IV). CLINI- tributed. Metabolized in liver. Primarily
CAL: Antianxiety, sedative-hypnotic, excreted in urine. Not removed by hemo-
antiemetic, skeletal muscle relax- dialysis. Half-life: 10–20 hrs.
ant, amnesiac, anticonvulsant, anti-
LIFESPAN CONSIDERATIONS
tremor.
Pregnancy/Lactation: May cross pla-
centa. May be distributed in breast milk.
USES May increase risk of fetal abnormalities
PO: Management of anxiety disorders, if administered during first trimester
short-term relief of symptoms of anxi- of pregnancy. Chronic ingestion during
ety, anxiety associated with depressive pregnancy may produce fetal toxicity,
symptoms. Insomnia due to anxiety or withdrawal symptoms, CNS depression
transient stress. IV: Status epilepticus, in neonates. Children: Safety and effi-
preanesthesia for amnesia, sedation. OFF- cacy not established in pts younger than
LABEL: Treatment of alcohol withdrawal, 12 yrs. Elderly: Use small initial doses
psychogenic catatonia, partial complex with gradual increases to avoid ataxia,
seizures, agitation (IV administration excessive sedation, or paradoxical CNS
only), antiemetic for chemotherapy; restlessness, excitement. May be more L
rapid tranquilization of agitated pt, status susceptible to cognitive impairment, de-
epilepticus in children. lirium, falls, fractures.

PRECAUTIONS INTERACTIONS
Contraindications: Hypersensitivity to LO- DRUG: Valproic acid may increase
Razepam, other benzodiazepines. Acute concentration/effects. Alcohol, other
narrow-angle glaucoma, severe respira- CNS depressants (e.g., morphine,
tory depression (except during mechani- PHENobarbital, zolpidem) may in-
cal ventilation). Cautions: Neonates, crease CNS depression. HERBAL: Herb-
renal/hepatic impairment, compromised als with sedative properties (e.g.,
pulmonary function, concomitant CNS chamomile, kava kava, valerian) may
depressant use, depression, history of increase CNS depression. FOOD: None
drug dependence, alcohol abuse, or sig- known. LAB VALUES: None significant.
nificant personality disorder, pts at risk Therapeutic serum level: 50–240 ng/
for suicide. mL; toxic serum level: unknown.

ACTION AVAILABILITY (Rx)


Enhances action of inhibitory neu- Injection Solution: 2 mg/mL, 4 mg/mL.
rotransmitter gamma-aminobutyric acid Oral Solution: (Lorazepam Intensol): 2
(GABA) in CNS, affecting memory, motor, mg/mL. Tablets: 0.5 mg, 1 mg, 2 mg.
sensory, cognitive function. Therapeutic
Effect: Produces anxiolytic, anticon- ADMINISTRATION/HANDLING
vulsant, sedative, muscle relaxant, anti- IV
emetic effects.
Reconstitution • Dilute with equal
PHARMACOKINETICS volume of Sterile Water for Injection,
Route Onset Peak Duration
D5W, or 0.9% NaCl.
Rate of administration • Give by IV
PO 30–60 min N/A 6–8 hrs
IV 5–20 min N/A 6–8 hrs
push into tubing of free-flowing IV infu-
IM 20–30 min N/A 6–8 hrs sion (0.9% NaCl, D5W) at a rate not to
exceed 2 mg/min.

Canadian trade name Non-Crushable Drug High Alert drug


718 LORazepam
Storage • Refrigerate parenteral form. SIDE EFFECTS
• Do not use if discolored or precipitate Frequent (16%–7%): Drowsiness, dizziness.
forms. • Avoid freezing. Rare (less than 4%): Weakness, ataxia,
IM headache, hypotension, nausea, vomiting,
• Give deep IM into large muscle mass. confusion, injection site reaction.

PO ADVERSE EFFECTS/TOXIC
• Give with food. • Tablets may be REACTIONS
crushed. • Dilute oral solution in wa- Abrupt or too-rapid withdrawal may re-
ter, juice, soda, or semisolid food. sult in pronounced restlessness, irritabil-
ity, insomnia, hand tremor, abdominal
IV INCOMPATIBILITIES cramping, muscle cramps, diaphoresis,
Aztreonam (Azactam), ondansetron (Zo­ vomiting, seizures. Overdose results in
fran). drowsiness, confusion, diminished re-
flexes, coma. Antidote: Flumazenil (see
IV COMPATIBILITIES Appendix J for dosage).
Bumetanide (Bumex), cefepime (Maxi-
pime), dexmedetomidine (Precedex), NURSING CONSIDERATIONS
dilTIAZem (Cardizem), DOBUTamine BASELINE ASSESSMENT
L
(Dobutrex), DOPamine (Intropin), hep- Offer emotional support to anxious pt. Pt
arin, labetalol (Normodyne, Trandate), must remain recumbent following paren-
milrinone (Primacor), norepinephrine teral administration to reduce ­hypotensive
(Levophed), piperacillin and tazo- effect. Assess motor responses (agitation,
bactam (Zosyn), potassium, propofol trembling, tension), autonomic responses
(Diprivan). (cold or clammy hands, diaphoresis).
INDICATIONS/ROUTES/DOSAGE INTERVENTION/EVALUATION
Anxiety Monitor B/P, respiratory rate, heart rate.
PO: ADULTS, ELDERLY: Initially, 0.5–1 mg For those on long-term therapy, hepatic/
2–3 times/day. May gradually increase renal function tests, CBC should be per-
up to 6 mg/day in 2–4 divided doses. formed periodically. Assess for paradoxical
reaction, particularly during early therapy.
Insomnia Due to Anxiety
Evaluate for therapeutic response: calm
PO: ADULTS: (less than 65 yrs): 0.5–2 facial expression, decreased restlessness,
mg at bedtime. (65 yrs and older): 0.5–1 insomnia, decrease in seizure-related
mg at bedtime. symptoms. Therapeutic serum level:
Status Epilepticus 50–240 ng/mL; toxic serum level: N/A.
IV: ADULTS, ELDERLY, CHILDREN:0.1 mg/ PATIENT/ FAMILY TEACHING
kg (maximum dose: 4 mg). Give at maxi- • Drowsiness usually subsides during
mum rate of 2 mg/min. May repeat in continued therapy. • Avoid tasks that re-
5–10 min. quire alertness, motor skills until re-
Dosage in Renal/Hepatic Impairment sponse to drug is established. • Smok-
PO: No dose adjustment. ing reduces drug effectiveness. • Do not
IM, IV: Mild to moderate impair- abruptly discontinue medication after
ment: Use caution. Not recommended long-term therapy. • Do not use alcohol,
in severe impairment. CNS depressants. • Contraception rec-
ommended for long-term therapy. • Im-
mediately report suspected pregnancy.

underlined – top prescribed drug


lorlatinib 719
ROS1, TYK1, FER, FPS, TRKA, TRKB,
lorlatinib TRKC, FAK, FAK2, and ACK). Also has ac-
tivity against cells expressing EML4-ALK.
lor-la-ti-nib Therapeutic Effect: Expresses antitu-
(Lorbrena) mor activity against ALK mutant forms in
Do not confuse lorlatinib with NSCLC in pts who have progressed with
alectinib, brigatinib, ceritinib, alectinib, ceritinib, or crizotinib.
crizotinib, erlotinib, lapatinib,
neratinib, lenvatinib, loratidine, PHARMACOKINETICS
or lorazepam. Widely distributed. Metabolized in liver.
Protein binding: 66%. Peak plasma con-
uCLASSIFICATION
centration: 1.2–2 hrs. Excreted in urine
PHARMACOTHERAPEUTIC: Anaplastic (48%), feces (41%). Half-life: 24 hrs.
lymphoma kinase inhibitor. Tyrosine
kinase inhibitor. CLINICAL: Antineo- LIFESPAN CONSIDERATIONS
plastic. Pregnancy/Lactation: Avoid preg-
nancy; may cause fetal harm. Female pts
of reproductive potential must use effec-
USES
tive nonhormonal contraception during
Treatment of pts with anaplastic lym- treatment and for at least 6 mos after dis- L
phoma kinase (ALK)–positive metastatic continuation. Hormonal contraception
non–small-cell lung cancer (NSCLC) may become ineffective with treatment.
whose disease has progressed on crizo- Unknown if distributed in breast milk.
tinib and at least one other ALK inhibitor Breastfeeding not recommended during
for metastatic disease; or progressed on treatment and for at least 7 days after
alectinib as the first ALK inhibitor therapy discontinuation. Males: Male pts with
for metastatic disease; or progressed on female partners of reproductive potential
ceritinib as the first ALK inhibitor therapy must use barrier methods during treat-
for metastatic disease. ment and for at least 3 mos after discon-
tinuation. May impair fertility. Children:
PRECAUTIONS
Safety and efficacy not established. El-
Contraindications: Hypersensitivity to lor- derly: No age-related precautions noted.
latinib. Concomitant use of strong CYP3
inducers. Cautions: Baseline anemia, INTERACTIONS
lymphopenia, thrombocytopenia; hyper- DRUG: Strong CYP3A4 inhibitors (e.g.,
lipidemia, cardiac or pulmonary disease, clarithromycin, ketoconazole) may
hepatic impairment, concomitant use of increase concentration/effect. Strong
strong or moderate CYP3A inhibitors, CYP3A4 inducers (e.g., carBAM-
moderate CYP3A inducers; pt at risk for azepine, phenytoin, rifAMPin) may
atrioventricular (AV) block (idiopathic decrease concentration/effect; use contra-
cardiac conduction disorders, ischemic indicated due to risk of severe hepatotox-
heart disease, increased vagal tone, con- icity. Moderate CYP3A inducers (e.g.,
comitant use of antiarrhythmics, beta bosentan, nafcillin) may decrease con-
blockers, calcium channel blockers); centration/effect. HERBAL: St. John’s wort
history of anxiety, depression, suicidal may decrease concentration/effect; use
ideation and behavior, mood disorder. contraindicated. FOOD: None known. LAB
VALUES: May increase serum alkaline phos-
ACTION
phatase, ALT, AST, amylase, cholesterol, glu-
Inhibits ALK phosphorylation, ALK down- cose, lipase, potassium, triglycerides. May
stream signaling proteins, multiple mu- decrease Hgb, lymphocytes, platelets, RBCs;
tant forms of ALK (activity against ALK, serum albumin, phosphate, magnesium.

Canadian trade name Non-Crushable Drug High Alert drug


720 lorlatinib

AVAILABILITY (Rx) Grade 4 CNS effects: Permanently


Tablets: 25 mg, 100 mg. discontinue.

ADMINISTRATION/HANDLING Hyperlipidemia
Grade 4 hypercholesterolemia or hy-
PO
pertriglyceridemia: Withhold treatment
• Give without regard to food. • Ad-
until improved to Grade 2 or less, then
minister tablets whole; do not break,
resume at same dose. Recurrent severe
crush, cut, or divide. Tablets cannot be
hypercholesterolemia or hypertri-
chewed. Do not give is tablet is broken,
glyceridemia: Resume at reduced dose.
cracked, or not intact. • If vomiting
occurs after administration, give next Interstitial Lung Disease (ILD)
dose at regularly scheduled time. • If a Any Grade treatment-related ILD:
dose is missed, administer as soon as Permanently discontinue.
possible. • Do not give a missed dose
within 4 hrs of next dose. Other Adverse Reactions
Any Grade 1 or Grade 2 Reaction:
INDICATIONS/ROUTES/DOSAGE Maintain dose or reduce dose.
Non–Small-Cell Lung Cancer Any Grade 3 or Grade 4 reaction:
PO: ADULTS, ELDERLY: 100 mg once daily. Withhold treatment until improved to Grade
L Continue until disease progression or un- 2 or less (or baseline), then resume at
acceptable toxicity. reduced dose.
Dose Reduction Schedule Concomitant Use of Strong CYP3A
First reduction: 75 mg once daily. Inhibitors
Second reduction: 50 mg once daily. If strong CYP3A inhibitor cannot be dis-
Unable to tolerate 50-mg dose: Per- continued, reduce dose to 75 mg. If dose
manently discontinue. was reduced to 75 mg due to adverse
reactions and a CYP3A inhibitor is
Dose Modification started, reduce dose to 50 mg. If CYP3A
Based on Common Terminology Criteria inhibitor is discontinued for 3 half-lives,
for Adverse Events (CTCAE). may resume dose prior to starting CYP3A
inhibitor.
Atrioventricular (AV) Block
Second-degree AV block: Withhold Concomitant Use of Moderate CYP3A
treatment until PR interval is less than 200 Inducers
msec, then resume at reduced dose. First Note: Concomitant use of strong CYP3A
occurrence of complete AV block: inducers is contraindicated.
Withhold treatment until PR interval is less If moderate CYP3A inducer cannot be
than 200 msec or pacemaker is placed. discontinued, consider discontinuing
If pacemaker is placed, resume at same CYP3A inducer or discontinuing treatment
dose. If pacemaker is not placed, resume if Grade 2 or higher hepatotoxicity occurs.
at reduced dose. Recurrent complete
AV block: Place pacemaker or perma- Dosage in Renal Impairment
nently discontinue. Mild to moderate impairment: No
dose adjustment. Severe impairment:
Central Nervous System (CNS) Effects Not specified; use caution.
Grade 1 CNS effects: Maintain dose
or withhold treatment until improved to Dosage in Hepatic Impairment
baseline, then resume at same dose or re- Mild impairment: No dose adjustment.
duced dose. Grade 2 or 3 CNS effects: Moderate to severe impairment: Not
Withhold treatment until improved to specified; use caution.
Grade 1 or 0, then resume at reduced dose.
underlined – top prescribed drug
lorlatinib 721

SIDE EFFECTS behavior; cardiac or pulmonary disease,


Frequent (57%–18%): Edema (general- hepatic impairment. Receive full medica-
ized, peripheral), peripheral neuropa- tion history and screen for interactions/
thy, cognitive effects (amnesia, memory contraindications. Conduct baseline neu-
impairment, disorientation), dyspnea, rologic exam. Offer emotional support.
fatigue, asthenia, weight gain, mood ef- INTERVENTION/EVALUATION
fects (aggression, agitation, anxiety,
Monitor CBC, LFTs periodically. Monitor
depression, mood swings), arthralgia,
serum cholesterol, triglycerides monthly
diarrhea, headache, cough, nausea. Oc-
for 2 mos, then periodically thereaf-
casional (17%–10%): Myalgia, dizziness,
ter. Monitor ECG periodically (or more
vision disorder, constipation, rash, back
frequently if symptoms of AV block oc-
pain, extremity pain, vomiting, speech ef-
cur [dizziness, chest pain, syncope]).
fects (aphasia, dysarthria), pyrexia, sleep
If moderate CYP3A inducer cannot be
effects (abnormal dreams, insomnia,
discontinued, monitor LFTs 48 hrs after
nightmares, sleep talking).
initiation and for at least 3 times during
ADVERSE EFFECTS/TOXIC the first week after initiation. Diligently
REACTIONS monitor for suicidal ideation and behav-
ior; new-onset or worsening of anxiety,
Anemia, lymphopenia, thrombocytope-
depression, mood disorder. Consider L
nia is an expected response to therapy.
mental health consultation if psychiat-
Concomitant use with moderate CYP3A
ric disorder suspected. Conduct regular
inducers my increase risk of hepatotox-
neurologic exams to rule out CNS effects.
icity. CNS reactions including hallucina-
Consider ABG, radiologic test if ILD/
tions, seizures, suicidal ideation, and
pneumonitis (excessive cough, dyspnea,
changes in cognitive function, mental
hypoxia) is suspected. If treatment re-
status, mood, sleep, speech reported in
lated toxicities occur, consider referral
54% of pts. Grade 3 or 4 elevations in
to specialist. Assess skin for rash, der-
total cholesterol, triglycerides reported
matitis.
in 18% of pts. AV block and PR internal
prolongation reported in 1% of pts. Life- PATIENT/FAMILY TEACHING
threatening ILD/pneumonitis reported in • Treatment may depress your immune
2% of pts. Other adverse effects, includ- system response and reduce your ability
ing pneumonia, pulmonary edema, myo- to fight infection. Report symptoms of
cardial infarction, embolism, peripheral infection such as body aches, chills,
artery occlusion, respiratory failure, oc- cough, fatigue, fever. Avoid those with
cur rarely. active infection. • Seek immediate
medical attention if thoughts of suicide,
NURSING CONSIDERATIONS new-onset or worsening of anxiety, de-
BASELINE ASSESSMENT pression, or changes in mood oc-
Obtain CBC, LFTs, serum cholesterol, tri- curs. • Neurologic events including al-
glycerides, ECG; pregnancy test in female tered speech, hallucinations, seizures
pts of reproductive potential. Verify ALK- may occur. • Report symptoms of heart
positive NSCLC status. Discontinue strong block (dizziness, chest pain, fainting);
CYP3A4 inducers for 3 half-lives prior to liver problems (abdominal pain, bruis-
initiation. Consider initiating or increas- ing, clay-colored stool, amber or dark
ing dose of antihyperlipidemic agents. colored urine, yellowing of the skin or
Confirm compliance of effective con- eyes); inflammation of the lung (exces-
traception. Screen for active infection. sive cough, difficulty breathing, chest
Question history of anxiety, depression, pain); skin reactions (rash). • Female
mood disorder, suicidal ideation and pts of childbearing potential must use

Canadian trade name Non-Crushable Drug High Alert drug


722 losartan
effective contraception during treatment PRECAUTIONS
and up to 6 mos after last dose. Do not Contraindications: Hypersensitivity to
breastfeed. Male pts with female partners losartan. Concomitant use of aliskiren in
of childbearing potential must use effec- pts with diabetes. Cautions: Renal/hepatic
tive contraception during treatment and impairment, unstented renal arterial ste-
for at least 3 mos after last dose. • There nosis, significant aortic/mitral stenosis.
is a high risk of interactions with other Concurrent use of potassium supplements.
medications. Do not take newly pre- Pts with history of angioedema.
scribed medications unless approved by
prescriber that originally started ther- ACTION
apy. • Avoid grapefruit products, herbal Blocks vasoconstrictor, aldosterone-
supplements (esp. St. John’s wort). secreting effects of angiotensin II, in-
hibiting binding of angiotensin II to AT1
receptors. Therapeutic Effect: Causes
losartan vasodilation, decreases peripheral resis-
tance, decreases B/P.
loe-sar-tan
(Cozaar) PHARMACOKINETICS
j BLACK BOX ALERT jMay Route Onset Peak Duration
L cause fetal injury, mortality. Dis- PO N/A 6 hrs 24 hrs
continue as soon as possible once
pregnancy is detected. Well absorbed after PO administration.
Do not confuse Cozaar with Col- Protein binding: 98%. Metabolized in
ace, Coreg, Hyzaar, or Zocor, or liver. Excreted in urine (35%), feces
losartan with lorcaserin, valsartan. (60%). Not removed by hemodialysis.
Half-life: 2 hrs; metabolite, 6–9 hrs.
FIXED-COMBINATION(S)
Hyzaar: losartan/hydroCHLOROthia- LIFESPAN CONSIDERATIONS
zide (a diuretic): 50 mg/12.5 mg, 100 Pregnancy/Lactation: Has caused fe-
mg/12.5 mg, 100 mg/25 mg. tal/neonatal morbidity, mortality. Potential
for adverse effects on breastfed infant.
uCLASSIFICATION
Breastfeeding not recommended. Chil-
PHARMACOTHERAPEUTIC: Angio- dren: Safety and efficacy not established.
tensin II receptor antagonist. CLINI- Elderly: May be more sensitive to hypo-
CAL: Antihypertensive. tensive effects.
INTERACTIONS
USES DRUG: NSAIDs (e.g., ibuprofen,
Treatment of hypertension in adults and ketorolac, naproxen) may decrease
children 6 yrs and older. Used alone effects. Aliskiren may increase hyper-
or in combination with other antihy- kalemic effect. May increase adverse/
pertensives. Treatment of diabetic ne- toxicity of ACE inhibitors (e.g., bena-
phropathy with an elevated creatinine zepril, lisinopril). May increase levels/
and proteinuria (in pts with type 2 effects of lithium. HERBAL: Herbals
diabetes and history of hypertension), with hypertensive properties (e.g.,
prevention of stroke in pts with hyper- licorice, yohimbe) or hypoten-
tension and left ventricular hypertrophy. sive properties (e.g., garlic, gin-
OFF-LABEL: Slow rate of progression ger, ginkgo biloba) may alter effects.
of aortic root dilation in children with FOOD: None known. LAB VALUES: May
Marfan’s syndrome. HF in pts intolerant increase serum bilirubin, ALT, AST, Hgb,
of ACE inhibitors. Hct. May decrease serum glucose.
underlined – top prescribed drug
lovastatin 723

AVAILABILITY (Rx) NURSING CONSIDERATIONS


Tablets: 25 mg, 50 mg, 100 mg.
BASELINE ASSESSMENT
ADMINISTRATION/HANDLING Obtain B/P, apical pulse immediately
PO before each dose, in addition to regular
• May give without regard to food. monitoring (be alert to fluctuations).
Question for possibility of pregnancy. As-
INDICATIONS/ROUTES/DOSAGE sess medication history (esp. diuretics).
Hypertension
INTERVENTION/EVALUATION
PO: ADULTS, ELDERLY: Initially, 25–50
mg once daily. May increase as needed Maintain hydration (offer fluids fre-
to 100 mg/day in 1–2 divided doses. quently). Assess for evidence of upper
CHILDREN 6–16 YRS: Initially, 0.7 mg/kg
respiratory infection, cough. Monitor
(maximum: 50 mg) once daily. Adjust B/P, pulse. Assist with ambulation if diz-
dose to BP response. Maximum: 1.4 ziness occurs. Monitor daily pattern of
mg/kg or 100 mg/day. bowel activity, stool consistency.
PATIENT/FAMILY TEACHING
Diabetic Nephropathy
PO: ADULTS, ELDERLY: Initially, 50 mg/ • Female pts of childbearing age should
day. May increase to 100 mg/day based take measures to avoid pregnancy. L
on B/P response. • Report pregnancy as soon as possi-
ble. • Avoid tasks that require alert-
Stroke Prevention (Hypertension with Left ness, motor skills until response to drug
Ventricular Hypertrophy) is established (possible dizziness ef-
PO: ADULTS, ELDERLY: Initially, 50 mg/ fect). • Report any sign of infection
day. Maximum: 100 mg/day based on (sore throat, fever), chest pain. • Do
BP response. Should be used in combi- not take OTC cold preparations, nasal
nation with a thiazide diuretic. decongestants. • Do not stop taking
medication. • Limit salt intake.
Dosage in Renal Impairment
Not recommended if glomerular filtration
rate (GFR) less than 30 mL/min.
lovastatin
Dosage in Hepatic Impairment
PO: ADULTS, ELDERLY: Initially, 25 mg/ loe-va-stat-in
day. May increase up to 100 mg/day. (Altoprev)
Do not confuse lovastatin
SIDE EFFECTS with atorvastatin, Leustatin,
Frequent (8%): Upper respiratory tract Lotensin, nystatin, pitavastatin,
infection. Occasional (4%–2%): Dizzi- or pravastatin, or Mevacor with
ness, diarrhea, cough. Rare (1% or less): Benicar or Lipitor.
Insomnia, dyspepsia, heartburn, back/
leg pain, muscle cramps, myalgia, nasal FIXED-COMBINATION(S)
congestion, sinusitis, depression. Advicor: lovastatin/niacin: 20 mg/500
mg, 20 mg/750 mg, 20 mg/1,000 mg.
ADVERSE EFFECTS/TOXIC
REACTIONS uCLASSIFICATION
Overdosage may manifest as hypotension PHARMACOTHERAPEUTIC: HMG-CoA
and tachycardia. Bradycardia occurs less reductase inhibitor. CLINICAL: Anti-
often. Institute supportive measures. hyperlipidemic.

Canadian trade name Non-Crushable Drug High Alert drug


724 lovastatin

USES LIFESPAN CONSIDERATIONS


Adjunct to diet to decrease elevated Pregnancy/Lactation: Contraindicated
serum total and LDL cholesterol in pri- in pregnancy (suppression of cholesterol
mary hypercholesterolemia; primary biosynthesis may cause fetal toxicity) and
prevention of coronary artery disease; lactation. Unknown if drug is distributed
reduction of risk of MI, unstable an- in breast milk. Children: Safety and ef-
gina, and in coronary revasculariza- ficacy not established. Elderly: No age-
tion procedures. Slows progression of related precautions noted.
coronary atherosclerosis in pts with
coronary heart disease. Adjunct to diet INTERACTIONS
in adolescent pts (10–17 yrs) with DRUG: Strong CYP3A4 inhibitors (e.g.,
heterozygous familial hypercholesterol- clarithromycin, ketoconazole, rito-
emia having LDL greater than 189 mg/ navir) may increase concentration, risk
dL or LDL greater than 160 mg/dL with of myopathy, rhabdomyolysis. Colchicine,
positive family history of premature CV gemfibrozil may increase risk of myopathy.
disease or LDL greater than 160 mg/dL HERBAL: St. John’s wort may decrease
with presence of at least 2 other CVD concentration/effects. FOOD: Large quanti-
risk factors. ties of grapefruit juice may increase risk
of side effects (e.g., myalgia, weakness).
L PRECAUTIONS Red yeast rice may increase concentration
Contraindications: Hypersensitivity to (2.4 mg lovastatin/600 mg rice). LAB VAL-
lovastatin. Active hepatic disease, unex- UES: May increase serum ALT, AST, creatine
plained persistent elevations of serum kinase (CK).
transaminases. Pregnancy, breastfeeding.
Concomitant use of strong CYP3A4 inhibi- AVAILABILITY (Rx)
tors. Cautions: History of heavy/chronic Tablets: 10 mg, 20 mg, 40 mg.
alcohol use, renal impairment, hepatic dis- Tablets: (Extended-Release [Alto-
ease; concomitant use of amiodarone, cy- prev]): 20 mg, 40 mg, 60 mg.
cloSPORINE, fibrates, gemfibrozil, niacin,
verapamil (increased risk of myopathy), ADMINISTRATION/HANDLING
elderly. PO
• Immediate-release tablet given with
ACTION evening meal; extended-release at bed-
Inhibits HMG-CoA reductase, the enzyme time. • Avoid intake of large quantities
that catalyzes the early step in cholesterol of grapefruit juice (greater than 1
synthesis. Therapeutic Effect: Decre­ quart). • Do not break, crush, dis-
a­ses LDL, VLDL, triglycerides; increases solve, or divide extended-release tablets.
HDL.
INDICATIONS/ROUTES/DOSAGE
PHARMACOKINETICS Hypercholesterolemia, Primary
Route Onset Peak Duration Prevention of CAD
PO (LDL, 3 days N/A N/A PO: (Immediate-Release): ADULTS, EL-
cholesterol DERLY: Initially, 20 mg/day. Adjust at 4-wk
reduction) intervals. Maintenance: 10–80 mg
once daily or in 2 divided doses. Maxi-
Incompletely absorbed from GI tract mum: 80 mg/day.
(increased on empty stomach). Protein PO: (Extended-Release): ADULTS, EL-
binding: 95%. Hydrolyzed in liver. Pri- DERLY: Initially, 20–60 mg once daily at
marily excreted in feces. Not removed by bedtime. Adjust at 4-wk intervals. Maxi-
hemodialysis. Half-life: 1.1–1.7 hrs. mum: 60 mg once daily at bedtime.

underlined – top prescribed drug


lurasidone 725
Heterozygous Familial pruritus. Monitor serum cholesterol,
Hypercholesterolemia triglycerides for therapeutic response.
PO: (Immediate-Release): CHIL- Be alert for malaise, muscle cramping/
DREN 10–17 YRS: (LDL reduction 20% weakness. Monitor LFT.
or greater): Initially, 20 mg/day; (LDL
reduction less than 20%): Initially, 10 PATIENT/FAMILY TEACHING
mg/day. Adjust at 4-wk intervals. Range: • Follow special diet (important part of
10–40 mg daily. treatment). • Periodic lab tests are
essential part of therapy. • Maintain
Dosage with Concurrent Medication appropriate birth control measures.
Amiodarone: Maximum: 40 mg/day. • Avoid grapefruit juice, alcohol. • Re-
DilTIAZem, dronedarone, verapamil: port severe gastric upset, vision changes,
Maximum: (Immediate-Release): 10 myalgia, weakness, changes in color of
mg/day. (Extended-Release): 20 mg/day. urine/stool, yellowing of eyes/skin, un-
Lomitapide: Consider reduction in dose. usual bruising.
Dosage in Renal Impairment
Use caution.
Dosage in Hepatic Impairment
lurasidone
No dose adjustment. L
loo-ras-i-done
SIDE EFFECTS (Latuda)
Generally well tolerated. Side effects usu- j BLACK BOX ALERT jElderly pts
with dementia-related psychosis
ally mild and transient. Frequent (9%– are at increased risk for mortal-
5%): Headache, flatulence, diarrhea, ity due to cardiovascular events,
abdominal pain, abdominal cramping, infectious diseases. Increased risk
rash, pruritus. Occasional (4%–3%): Nau- of suicidal thinking/behavior in chil-
sea, vomiting, constipation, dyspepsia. dren, adolescents, young adults.
Rare (2%–1%): Dizziness, heartburn, my-
uCLASSIFICATION
algia, blurred vision, eye irritation.
PHARMACOTHERAPEUTIC: DOPa-
ADVERSE EFFECTS/TOXIC mine, serotonin receptor antagonist.
REACTIONS CLINICAL: Second-generation (atyp-
Potential for cataract development. Occa- ical) antipsychotic.
sionally produces myopathy manifested
as muscle pain, tenderness, weakness
with elevated creatine kinase (CK). Severe USES
myopathy may lead to rhabdomyolysis. Treatment of schizophrenia in adults and
adolescents (13–17 yrs). Treatment of
NURSING CONSIDERATIONS depression associated with bipolar I dis-
BASELINE ASSESSMENT order as monotherapy (children 10 yrs
and older, adults) and as adjunctive ther-
Obtain dietary history. Question for pos- apy (adults) with lithium or valproate.
sibility of pregnancy before initiating
therapy. Obtain LFT, serum cholesterol, PRECAUTIONS
triglycerides. Contraindications: Hypersensitivity to
INTERVENTION/EVALUATION lura­
sidone. Concurrent use with strong
Monitor daily pattern of bowel activity, CYP3A4 inhibitors (e.g., ketoconazole)
stool consistency. Monitor for headache, and inducers (e.g., rifAMPin). Cautions:
dizziness, blurred vision. Assess for rash, Cardiovascular disease (HF, history of MI,
ischemia, conduction abnormalities),
Canadian trade name Non-Crushable Drug High Alert drug
726 lurasidone
cerebrovascular disease (history of CVA products may increase concentration/
in pts with dementia, seizure disorders), effect. LAB VALUES: May increase pro-
diabetes, Parkinson’s disease, renal/hepatic lactin levels.
impairment, pts at risk for aspiration pneu-
monia, pts at risk for suicide, disorders AVAILABILITY (Rx)
where CNS depression is a feature, pts at Tablets: 20 mg, 40 mg, 60 mg, 80 mg,
risk for hypotension, elderly, head trauma, 120 mg.
alcoholism, medications that lower seizure
threshold. ADMINISTRATION/HANDLING
PO
ACTION • Give with food. • Tablets may be
Antagonizes central DOPamine type 2 and crushed.
serotonin type 2 receptors. Therapeutic
Effect: Diminishes symptoms of schizo- INDICATIONS/ROUTES/DOSAGE
phrenia. Reduces incidence of extrapyra- Schizophrenia
midal side effects. PO: ADULTS, ELDERLY: Initially, 40 mg once
daily with food. Increase dose based on re-
PHARMACOKINETICS sponse and tolerability. Maximum: 160 mg
Absorbed in 1–3 hrs. Steady-state con- once daily with food. ADOLESCENTS: Initially,
L centration occurs in 7 days. Well ab- 40 mg once daily with food. Maximum: 80
sorbed from GI tract (unaffected by mg once daily with food.
food). Protein binding: 99%. Metabo-
lized in liver. Excreted in feces (80%), Bipolar Depression
urine (9%). Half-life: 18 hrs. PO: ADULTS, ELDERLY: (Monotherapy
or adjunct to lithium or dival-
LIFESPAN CONSIDERATIONS proex): Initially, 20 mg once daily,
Pregnancy/Lactation: Unknown if dis- alone or in combination with lithium
tributed in breast milk. Breastfeeding not or divalproex. May increase in 20
recommended. Children: Safety and ef- mg increments q2–7 days. Maxi-
ficacy not established. Elderly: More sus- mum: 120 mg/day. CHILDREN 10 YRS AND
OLDER: (Monotherapy): Initially, 20 mg
ceptible to postural hypotension. Increased
risk of cerebrovascular events (includ- once daily. May increase dose after 1
ing stroke), mortality, in elderly pts with wk. Maximum: 80 mg/day.
psychosis. Concomitant Use of Moderate CYP3A4
Inhibitors/Inducers
INTERACTIONS PO: ADULTS, ELDERLY: (Inhibitor): Ini-
DRUG: Alcohol, CNS depressants tially, 20 mg/day. Maximum: 80 mg/
(e.g., LORazepam, morphine, zolpi- day. (Inducer): May need to increase
dem) may increase CNS depression. May lurasidone dose if inducer used for 7 or
enhance CNS depressant effect of azelas- more days.
tine (nasal). Strong CYP3A4 induc-
ers (e.g., carBAMazepine, phenytoin, Moderate to Severe Renal Impairment
rifAMPin) decrease concentration/ef- CrCl less than 50 mL/min: Initially,
fects. Strong CYP3A4 inhibitors (e.g., 20 mg/day. Maximum: 80 mg/day.
clarithromycin, ketoconazole, rito-
navir) may increase concentration/ef- Hepatic Impairment
fects. HERBAL: Herbals with sedative Mild impairment: No dose adjust-
properties (e.g., chamomile, kava ment. Moderate impairment: Initially,
kava, valerian) may increase CNS de- 20 mg/day. Maximum: 80 mg/day. Se-
pression. St. John’s wort may decrease vere impairment: Initially, 20 mg/day.
concentration/effect. FOOD: Grapefruit Maximum: 40 mg/day.
underlined – top prescribed drug
lurasidone 727

SIDE EFFECTS pattern, thought content. Renal function,


Frequent (15%–7%): Drowsiness, seda- LFT should be obtained before therapy as
tion, insomnia (paradoxical reaction). dose adjustment is required when initiat-
Occasional (6%–3%): Nausea, vomiting, ing therapy.
dyspepsia, fatigue, back pain, akathisia, INTERVENTION/EVALUATION
dizziness, agitation, anxiety. Rare (2%–
Supervise suicidal risk pt closely during
1%): Restlessness, salivary hypersecre-
early therapy (as depression lessens,
tion, tongue spasm, torticollis, trismus.
energy level improves, increasing sui-
ADVERSE EFFECTS/TOXIC cide potential). Monitor for potential
REACTIONS neuroleptic malignant syndrome. Assess
for therapeutic response (greater inter-
Extrapyramidal disorder (including cog-
est in surroundings, improved self-care,
wheel rigidity, drooling, bradykinesia,
increased ability to concentrate, relaxed
tardive dyskinesia, tremors) occurs in
facial expression).
5% of pts. Neuroleptic malignant syn-
drome (fever, muscle rigidity, irregular PATIENT/FAMILY TEACHING
B/P or pulse, altered mental status, visual • Avoid tasks that may require alertness,
changes, dyspnea) occurs rarely. motor skills until response to drug is estab-
lished (may cause drowsiness, dizziness). L
NURSING CONSIDERATIONS • Avoid alcohol. • Report trembling in
fingers, altered gait, unusual muscle/
BASELINE ASSESSMENT skeletal movements, palpitations, severe
Question history as listed in Precautions. dizziness, fainting, visual changes, rash, dif-
Assess behavior, appearance, emotional ficulty breathing. • Report suicidal ide-
status, response to environment, speech ation, unusual changes in behavior.

Canadian trade name Non-Crushable Drug High Alert drug


728  magnesium

mia; prevention and treatment of seizures


magnesium in severe preeclampsia or eclampsia; pedi-
atric acute nephritis, treatment of arrhyth-
mag-nee-zee-um mias due to hypomagnesemia (ventricular
magnesium chloride fibrillation, ventricular tachycardia, or
torsades de pointes). OFF-LABEL: Magne-
(Mag-Delay, Slow-Mag) sium sulfate: Asthma exacerbation unre-
sponsive to conventional treatment.
magnesium citrate
PRECAUTIONS
(Citroma, Citro-Mag ) Contraindications: Antacid: Appendicitis,
symptoms of appendicitis, ileostomy, intes-
magnesium hydrox- tinal obstruction, severe renal impairment.
ide Laxative: Appendicitis, HF, colostomy, hy-
persensitivity, ileostomy, intestinal obstruc-
(Milk of Magnesia) tion, undiagnosed rectal bleeding. Sys-
temic: Heart block, myocardial damage,
magnesium oxide IV use for pre-eclampsia/eclampsia during
the 2 hrs prior to delivery. Cautions: Safety
(Mag-Ox 400, Uro-Mag) in children younger than 6 yrs not known.
Antacids: Undiagnosed GI/rectal bleed-
M magnesium sulfate ing, ulcerative colitis, colostomy, diverticuli-
tis, chronic diarrhea. Laxative: Diabetes,
(Epsom salt, magnesium sulfate in- pts on low-salt diet (some products contain
jection) sugar, sodium). Systemic: Severe renal
Do not confuse magnesium impairment. Myasthenia gravis or other
sulfate with morphine sulfate. neuromuscular diseases.
FIXED-COMBINATION(S) ACTION
With aluminum and simethicone, an Antacid: Acts in stomach to neutralize gas-
antiflatulent (Mylanta). tric acid. Therapeutic Effect: Increases
uCLASSIFICATION
pH. Laxative: Osmotic effect primarily in
small intestine, draws water into intestinal
CLINICAL: Antacid, anticonvulsant, lumen. Therapeutic Effect: Promotes
electrolyte, laxative. peristalsis, bowel evacuation. Systemic
(dietary supplement replacement):
USES Found primarily in intracellular fluids.
Therapeutic Effect: Essential for enzyme
Magnesium chloride: Treatment/pre- activity, nerve conduction, muscle contrac-
vention of hypomagnesemia. Dietary sup- tion. Maintains and restores magnesium
plement. Magnesium citrate: Evacuation levels. Anticonvulsant: Blocks neuromus-
of bowel before surgical, diagnostic proce- cular transmission, amount of acetylcholine
dures. Relieves occasional constipation. released at motor end plate. Therapeutic
Magnesium hydroxide: Short-term Effect: Produces seizure control.
treatment of constipation, symptoms of
hyperacidity, laxative. Magnesium oxide: PHARMACOKINETICS
Relief of acid indigestion and upset stom- Antacid, laxative: Minimal absorption
ach, short-term relief of constipation. Di- through intestine. Absorbed dose primar-
etary supplement. Magnesium sulfate: ily excreted in urine. Systemic: Widely
Treatment/prevention of hypomagnese- distributed. Primarily excreted in urine.

underlined – top prescribed drug


magnesium 729

LIFESPAN CONSIDERATIONS Rate of administration • For IV


Pregnancy/Lactation: Antacid: push (diluted): Give no faster than 150
Unknown if distributed in breast milk. mg/min. For IV infusion, maximum rate
Parenteral: Readily crosses placenta. of infusion is 2 g/hr.
Storage • Store at room temperature.
Distributed in breast milk for 24 hrs
after magnesium therapy is discontinued. IM
Continuous IV infusion increases risk of • For adults, elderly, use 250 mg/mL
magnesium toxicity in neonate. IV admin- (25%) or 500 mg/mL (50%) magnesium
istration should not be used 2 hrs preced- sulfate concentration. • For infants, chil-
ing delivery. Children: No age-related dren, do not exceed 200 mg/mL (20%
precautions noted. Elderly: Increased diluted solution).
risk of developing magnesium deficiency
(e.g., poor diet, decreased absorption, PO (Antacid)
medications). • Shake suspension well before use.
• Chewable tablets should be chewed
INTERACTIONS thoroughly before swallowing, followed
DRUG: May decrease absorption of by full glass of water.
quinolones (e.g., ciprofloxacin,
levoFLOXacin), tetracycline, bisphos- PO (Laxative)
phonates. HERBAL: None significant. • Drink full glass of liquid (8 oz) with
FOOD: None known. LAB VALUES: Ant- each dose (prevents dehydration).
acid: May increase gastrin production, • Flavor may be improved by following M
pH. Laxative: May decrease serum potas- with fruit juice, citrus carbonated bever-
sium. Systemic: None significant. age. • Refrigerate citrate of magnesia
(retains potency, palatability).
AVAILABILITY (Rx)
MAGNESIUM CHLORIDE IV INCOMPATIBILITIES
Tablets: (Mag-Delay, Slow-Mag): 64 mg. Amphotericin B complex (Abelcet, AmBi-
MAGNESIUM CITRATE some, Amphotec), cefepime (Maxipime),
Oral Solution: (Citroma): 290 mg/5 mL. lansoprazole (Prevacid), pantoprazole
Tablets: 100 mg. (Protonix).
MAGNESIUM HYDROXIDE
Suspension, Oral: (Milk of Magne- IV COMPATIBILITIES
sia): 400 mg/5 mL, 1,200 mg/15 mL. Amikacin (Amikin), ceFAZolin (Ancef),
Tablets: 400 mg. ciprofloxacin (Cipro), dexmedetomidine
MAGNESIUM OXIDE (Precedex), DOBUTamine (Dobutrex),
Capsules: (Uro-Mag): 140 mg. Tablets: enalapril (Vasotec), gentamicin, heparin,
(Mag-Ox 400): 400 mg. HYDROmorphone (Dilaudid), insulin, line-
MAGNESIUM SULFATE zolid (Zyvox), metoclopramide (Reglan),
Infusion Solution: 10 mg/mL, 20 mg/mL, milrinone (Primacor), morphine, piper-
40 mg/mL, 80 mg/mL. Injection Solution: acillin/tazobactam (Zosyn), potassium
125 mg/mL, 500 mg/mL. chloride, propofol (Diprivan), tobramycin
(Nebcin), vancomycin (Vancocin).
ADMINISTRATION/HANDLING
INDICATIONS/ROUTES/DOSAGE
IV
MAGNESIUM SULFATE
Reconstitution • Must dilute to maxi- Hypomagnesemia
mum concentration of 20% for IV infu- Mild to Moderate
sion. May give IV push, IV piggyback, or IV: ADULTS, ELDERLY: 1–4 g as 1 g/hr.
continuous infusion. Maximum: 12 g/12 hrs.

Canadian trade name Non-Crushable Drug High Alert drug


730  magnesium
Severe Deficiency SIDE EFFECTS
IV: ADULTS, ELDERLY: 4–8 g as 1 g/hr.
Frequent: Antacid: Chalky taste, diar-
IV: CHILDREN: 25–50 mg/kg/dose over
rhea, laxative effect. Occasional: Ant-
10–20 min. Maximum single dose: acid: Nausea, vomiting, stomach
2 g. cramps. Antacid, laxative: Prolonged
use or large doses in renal impair-
Usual Dose for Neonates
ment may cause hypermagnesemia
IM/IV: 25–50 mg/kg/dose q8–12h for (dizziness, palpitations, altered mental
2–3 doses. status, fatigue, weakness). Laxative:
Cramping, diarrhea, increased thirst,
Eclampsia/Preeclampsia
flatulence. Systemic (dietary supple-
IV: ADULTS: 4–6 g loading dose over ment, electrolyte replacement):
20–30 min, then 1–2 g/hr continuous Reduced respiratory rate, decreased
infusion. Maximum: 40 g/24 hrs. reflexes, flushing, hypotension,
decreased heart rate.
MAGNESIUM CHLORIDE
Dietary Supplement ADVERSE EFFECTS/TOXIC
PO: ADULTS, ELDERLY: 2 tablets once REACTIONS
daily. Magnesium as antacid, laxative has no
known adverse reactions. Systemic use
MAGNESIUM CITRATE
may produce prolonged PR interval, wid-
M Laxative
ening of QRS interval. Magnesium toxicity
PO: ADULTS, ELDERLY, CHILDREN 12 YRS
may cause loss of deep tendon reflexes,
AND OLDER: 195–300 mL once or in
heart block, respiratory paralysis, cardiac
divided doses. 6–12 YRS: 100–150 mL
arrest. Antidote: 10–20 mL 10% calcium
once or in divided doses. 2–5 YRS: 60–90
gluconate (5–10 mEq of calcium).
mL once or in divided doses.
MAGNESIUM HYDROXIDE
NURSING CONSIDERATIONS
Antacid BASELINE ASSESSMENT
PO: ADULTS, ELDERLY, CHILDREN 12 YRS Assess sensitivity to magnesium. Ant-
AND OLDER: (400 mg/5 mL): 5–15 mL acid: Assess GI pain (duration, lo-
as needed up to 4 times/day. cation, quality, time of occurrence,
Laxative relief with food, causative/exacerba-
PO: ADULTS, ELDERLY, CHILDREN 12 YRS tive factors). Laxative: Assess for
AND OLDER: (400 mg/5 mL): 30–60 weight loss, nausea, vomiting, history
mL at HS or in divided doses. (Tablet): of recent abdominal surgery. Sys-
8 tabs/day in divided doses.CHILDREN temic: Assess renal function, serum
6–11 YRS: (400 mg/5 mL): 15–30 magnesium.
mL at HS. CHILDREN 2–5 YRS: 5–15 mL INTERVENTION/EVALUATION
at HS.
Antacid: Assess for relief of gastric
MAGNESIUM OXIDE distress. Monitor renal function (esp.
if dosing is long term or frequent).
Antacid/Dietary Supplement
Laxative: Monitor daily pattern of
PO: ADULTS, ELDERLY: 1–2 tablets daily.
bowel activity, stool consistency. Main-
Dosage in Renal Impairment tain adequate fluid intake. Systemic:
Use caution. Monitor renal function, magnesium
levels, ECG for cardiac function.
Dosage in Hepatic Impairment Test patellar reflexes before giving re-
No dose adjustment. peated, rapid parenteral doses (used as

underlined – top prescribed drug


mannitol 731

indication of CNS depression; suppressed PRECAUTIONS


reflexes may be sign of impending respi- Contraindications: Hypersensitivity to man-
ratory arrest). Patellar reflex must be nitol. Severe dehydration, active intracra-
present, respiratory rate should be 16/ nial bleeding (except during craniotomy),
min or over before each parenteral dose. severe pulmonary edema, congestion,
Initiate seizure precautions. severe renal disease (anuria), progressive
HF. Cautions: Concurrent nephrotoxic
PATIENT/FAMILY TEACHING
agents, conditions increasing sensitiv-
• Antacid: Take at least 2 hrs apart ity to bronchoconstriction (e.g., recent
from other medication. • Do not take abdominal, thoracic surgery), sepsis,
longer than 2 wks unless directed by preexisting renal disease, hyperna­tremia.
physician. • For peptic ulcer, take 1
and 3 hrs after meals and at bedtime ACTION
for 4–6 wks. • Chew tablets thor- Increases osmotic pressure of glomeru-
oughly, followed by 8 oz of water; lar filtrate, inhibiting tubular reabsorp-
shake suspensions well. • Repeat tion of water and electrolytes, resulting
dosing or large doses may have laxative in increased urine output. Reduces intra-
effect. • Laxative: Drink full glass (8 cranial pressure by decreasing blood
oz) liquid to aid stool soften- viscosity, thereby increasing cerebral
ing. • Use only for short term. Do not blood flow/oxygen transport. Thera-
use if abdominal pain, nausea, vomit- peutic Effect: Produces diuresis;
ing is present. • Systemic: Report reduces intraocular pressure (IOP), M
symptoms of hypermagnesemia (al- intracranial pressure (ICP), cerebral
tered mental status, difficulty breath- edema.
ing, dizziness, fatigue, palpitations,
weakness). PHARMACOKINETICS
Route Onset Peak Duration
IV (diuresis) 1–3 hrs N/A —
IV (reduced 15–30 N/A 1.5–6 hrs
ICP) min
mannitol Remains in extracellular fluid. Primarily
excreted unchanged in urine. Removed
man-it-ol by hemodialysis. Half-life: 4.7 hrs.
(Resectisol, Osmitrol)
Do not confuse Osmitrol with LIFESPAN CONSIDERATIONS
esmolol. Pregnancy/Lactation: Unknown if
uCLASSIFICATION drug crosses placenta or is distributed in
breast milk. Children: Safety and efficacy
PHARMACOTHERAPEUTIC: Polyol
not established in pts younger than 12 yrs.
(sugar alcohol). CLINICAL: Osmotic Elderly: Age-related renal impairment
diuretic. may require dosage adjustment.
INTERACTIONS
USES
DRUG: May increase nephrotoxic effect
Reduces increased ICP due to cerebral
of aminoglycosides (e.g., amika-
edema, IOP due to acute glaucoma.
cin, tobramycin). HERBAL: None
Promotes urinary excretion of toxic
significant. FOOD: None known. LAB
substances. OFF-LABEL: Improves renal
VALUES: May decrease serum phos-
transplant function. Severe, traumatic
phate, potassium. May increase serum
brain injury.
sodium, serum osmolality.

Canadian trade name Non-Crushable Drug High Alert drug


732 mannitol

AVAILABILITY (Rx) Dosage in Renal Impairment


Injection Solution: (Osmitrol): 5%, 10%, Contraindicated with severe impairment;
15%, 20%, 25%. caution with underlying renal disease.
Dosage in Hepatic Impairment
ADMINISTRATION/HANDLING
No dose adjustment.
b ALERT c Assess IV site for patency
before each dose. Pain, thrombosis SIDE EFFECTS
noted with extravasation. In-line filter Frequent: Dry mouth, thirst. Occasional:
(less than 5 microns) used for concen- Blurred vision, increased urinary fre-
trations over 20%. quency/volume, headache, arm pain,
IV backache, nausea, vomiting, urticaria, diz-
ziness, hypotension, hypertension, tachy-
Rate of administration • Administer cardia, fever, angina-like chest pain.
test dose for pts with oliguria. • Give IV
push over 3–5 min; over 30–60 min for ADVERSE EFFECTS/TOXIC
cerebral edema, elevated ICP. Maximum REACTIONS
concentration: 25%. • Do not add KCl Fluid, electrolyte imbalance may occur
or NaCl to mannitol 20% or greater. Do due to rapid administration of large
not add to whole blood for transfusion. doses or inadequate urine output
Storage • Store at room tempera- resulting in overexpansion of extracel-
ture. • If crystals are noted in solution, lular fluid. Circulatory overload may
M warm bottle in hot water, shake vigor- produce pulmonary edema, HF. Exces-
ously at intervals. Cool to body tempera- sive diuresis may produce hypokale-
ture before administration. Do not use if mia. Fluid loss in excess of electrolyte
crystals remain after warming proce- excretion may produce hypernatremia,
dure. hyperkalemia.
IV INCOMPATIBILITIES NURSING CONSIDERATIONS
Cefepime (Maxipime), filgrastim (Neupo-
BASELINE ASSESSMENT
gen), imipenem-cilastatin (Primaxin).
Obtain serum osmolality, sodium. Ob-
IV COMPATIBILITIES tain baseline B/P, pulse. Assess skin tur-
CISplatin (Platinol), furosemide (Lasix), gor, mucous membranes, mental status,
linezolid (Zyvox), ondansetron (Zofran), muscle strength. Obtain baseline weight.
propofol (Diprivan). Assess hydration status.
INTERVENTION/EVALUATION
INDICATIONS/ROUTES/DOSAGE
USUAL DOSAGE
Monitor urinary output to ascertain
Elevated Intracranial Pressure
therapeutic response. Monitor serum
IV: ADULTS, ELDERLY: 0.25–1 g/kg/dose. electrolytes, serum osmolality, ICP, re-
May repeat q6–8h as needed to maintain nal function, LFT. Assess vital signs,
serum osmolality <300–325 mOsm/ skin turgor, mucous membranes. Weigh
kg. CHILDREN: 0.25–1 g/kg/dose; repeat daily. Monitor for signs of hypernatre-
to maintain serum osmolality <300–320 mia (confusion, drowsiness, thirst, dry
mOsm/kg. mouth, cold/clammy skin); signs of hy-
pokalemia (changes in muscle strength,
IOP Reduction tremors, muscle cramps, altered mental
IV: ADULTS, ELDERLY: 1.5–2 g/kg over status, cardiac arrhythmias). Signs of
30–60 min 1–1.5 hrs prior to surgery. hyperkalemia include colic, diarrhea,
CHILDREN: 1–2 g/kg over 30–60 min muscle twitching followed by weakness,
1–1.5 hrs prior to surgery. paralysis, arrhythmias.

underlined – top prescribed drug


medroxyPROGESTERone 733

PATIENT/FAMILY TEACHING (known, suspected or prior history),


history of or active thrombotic disorders
• Expect increased urinary frequency/ (thrombophlebitis, thromboembolic dis-
volume. • May cause dry mouth. orders), known or suspected pregnancy,
severe hepatic impairment, undiagnosed
abnormal vaginal bleeding, cerebrovascu-
medroxyPROGES- lar disease. Cautions: Pts with conditions
aggravated by fluid retention (asthma,
TERone seizures, migraine, cardiac/renal dysfunc-
tion), diabetes, history of mental depres-
me-drox-ee-proe-jes-ter-one sion, preexisting hypercholesterolemia,
(Depo-Provera, Depo-SubQ Provera hypertriglyceridemia.
104, Provera)
j BLACK BOX ALERT jProlonged ACTION
use (over 2 yrs) of contraceptive Inhibits secretion of pituitary gonado-
injection form may result in loss tropins. Therapeutic Effect: Prevents
of bone mineral density. Limit
long-term use (more than 2 yrs). follicular maturation, ovulation. Causes
May increase risk of dementia in endometrial thinning.
postmenopausal women. Increased
risk of invasive breast cancer in PHARMACOKINETICS
postmenopausal women in combi- Well absorbed after PO administration.
nation with conjugated estrogens.
Slowly absorbed after IM administration. M
Do not confuse medroxyPRO-
Protein binding: 90%. Metabolized in
GESTERone with HYDROXYpro-
liver. Primarily excreted in urine. Half-
gesterone, methylPREDNISo-
life: PO: 12–17 hrs. IM: 40–50 days.
lone, or methylTESTOSTERone,
or Provera with Covera, Femara, LIFESPAN CONSIDERATIONS
Parlodel, or Premarin.
Pregnancy/Lactation: Avoid use dur-
uCLASSIFICATION ing pregnancy, esp. first 4 mos (congenital
heart, limb reduction defects may occur).
PHARMACOTHERAPEUTIC: Hor-
Distributed in breast milk. Children: Safety
mone. CLINICAL: Progestin, antineo-
and efficacy not established. Elderly: No
plastic, contraceptive hormone.
age-related precautions noted.

USES INTERACTIONS
PO: Reduction of endometrial hyper- DRUG: Strong CYP3A inducers (e.g.,
plasia in nonhysterectomized postmeno- carBAMazepine, phenytoin, rifAMPin)
pausal women (concurrently given with may decrease effects. HERBAL: St. John’s
estrogen to women with intact uterus), wort may decrease effect of progestin con-
treatment of secondary amenorrhea, traceptive. Herbals with progestogenic
abnormal uterine bleeding due to hor- properties (e.g., bloodroot, chaste-
monal imbalance. IM: Adjunctive therapy, berry, yucca) may increase adverse effects.
FOOD: None known. LAB VALUES: May
palliative treatment of inoperable, recur-
rent, metastatic endometrial carcinoma; alter serum thyroid, LFT, PT, HDL, total cho-
prevention of pregnancy, endometriosis- lesterol, triglycerides; metapyrone test. May
associated pain. OFF-LABEL: Treatment of increase LDL.
paraphilia/hypersexuality. AVAILABILITY (Rx)
PRECAUTIONS Injection Suspension: (Depo-SubQ Provera
Hypersensitivity
Contraindications: to 104): 104 mg/0.65 mL prefilled syringe.
medroxyPROGESTERone. Breast cancer
Canadian trade name Non-Crushable Drug High Alert drug
734 medroxyPROGESTERone
(Depo-Provera): 150 mg/mL, 400 mg/mL. Dosage in Hepatic Impairment
Tablets: (Provera): 2.5 mg, 5 mg, 10 mg. Contraindicated with severe impairment.

ADMINISTRATION/HANDLING SIDE EFFECTS


IM Frequent: Transient menstrual abnormali-
• Shake vial immediately before admin- ties (spotting, change in menstrual flow/
istering (ensures complete suspen- cervical secretions, amenorrhea) at initia-
sion). • Administer deep IM into glu- tion of therapy. Occasional: Edema, weight
teal or deltoid muscle. change, breast tenderness, anxiety, insom-
nia, fatigue, dizziness. Rare: Alopecia,
SQ depression, dermatologic changes, head-
• Shake vigorously prior to administra- ache, fever, nausea.
tion. • Inject in upper thigh or abdo-
men (avoid bony areas and umbili- ADVERSE EFFECTS/TOXIC
cus). • Give over 5–7 sec; do not rub REACTIONS
injection area. Thrombophlebitis, pulmonary/cerebral
embolism, retinal thrombosis occur
PO rarely.
• Give with food.
NURSING CONSIDERATIONS
INDICATIONS/ROUTES/DOSAGE
Endometrial Hyperplasia BASELINE ASSESSMENT
M
PO: ADULTS: 5–10 mg/day for 12–14 Obtain usual menstrual history. Ques-
consecutive days each month starting on tion for hypersensitivity to progestins,
day 1 or 16 of cycle. possibility of pregnancy before initiating
therapy. Obtain baseline weight, serum
Secondary Amenorrhea glucose, B/P.
PO: ADULTS: 5–10 mg/day for 5–10
days, beginning at any time during men- INTERVENTION/EVALUATION
strual cycle. Check weight daily; report wkly gain of
5 lb or more. Assess B/P periodically.
Abnormal Uterine Bleeding Assess skin for rash, urticaria. Report
PO: ADULTS: 5–10 mg/day for 5–10 days, development of chest pain, sudden short-
beginning on calculated day 16 or day 21 of ness of breath, sudden decrease in vi-
menstrual cycle. sion, migraine headache, pain (esp. with
swelling, warmth, redness) in calves,
Endometrial Carcinoma numbness of arm/leg (thrombotic disor-
IM: ADULTS, ELDERLY: Initially, 400– ders) immediately.
1,000 mg; repeat at 1-wk intervals.
PATIENT/FAMILY TEACHING
Pregnancy Prevention • Report sudden loss of vision, severe
IM: (Depo-Provera): ADULTS: 150 mg headache, chest pain, coughing up of
q3mos (q13 wks). blood (hemoptysis), numbness in arm/
SQ: (Depo-Subq Provera 104): ADULTS: leg, severe pain/swelling in calf, un-
104 mg q3mos (q12–14wks). usually heavy vaginal bleeding, severe
Endometriosis
abdominal pain/tenderness. • Depo-
SQ: (Depo-Subq Provera 104): ADULTS:
Provera Contraceptive injection should
104 mg q3mos (q12–14 wks). ADULTS: be used as long-term birth control
method (e.g., longer than 2 yrs) only if
Dosage in Renal Impairment other birth control methods are inad-
No dose adjustment. equate.

underlined – top prescribed drug


megestrol 735

INTERACTIONS
megestrol DRUG: May decrease effects of antico-
agulants (e.g., warfarin). May increase
meh-jes-trol
concentration/effect of dofetilide.
(Megace ES, Megace OS )
HERBAL: Avoid black cohosh, dong
Do not confuse megestrol with
quai in estrogen-dependent tumors. Avoid
mesalamine.
herbs with progestogenic properties
uCLASSIFICATION (e.g., bloodroot, chasteberry, yucca);
may increase adverse effects. FOOD: None
PHARMACOTHERAPEUTIC: Synthetic
known. LAB VALUES: May alter serum thy-
hormone. CLINICAL: Antineoplastic,
roid, LFT, PT, HDL, total cholesterol, triglyc-
progestin, appetite stimulant.
erides. May increase LDL.

USES AVAILABILITY (Rx)


Oral Suspension: (Megace ES): 40 mg/mL,
Palliative treatment of advanced endome-
trial or breast carcinoma; treatment of 625 mg/5 mL. Tablets: 20 mg, 40 mg.
anorexia, cachexia, unexplained signifi- ADMINISTRATION/HANDLING
cant weight loss in pts with AIDS.
PO
PRECAUTIONS • Store tablets, oral suspension at room
Contraindications: Hypersensitivity to temperature. • Shake suspension well
before use. • Oral suspension compatible M
megestrol. Suspension: Known or
suspected pregnancy. Cautions: His- with water, orange juice, apple juice. • Ad-
tory of thrombophlebitis, elderly. minister without regard to food.

ACTION INDICATIONS/ROUTES/DOSAGE
Palliative Treatment of Advanced Breast
Antiestrogenic; interferes with normal
Cancer
estrogen cycle by decreasing release of
PO: ADULTS, ELDERLY: 40 mg 4 times/
luteinizing hormone (LH) from anterior
pituitary gland by inhibiting pituitary day for at least 2 mos.
function. Antineoplastic effect may act Palliative Treatment of Advanced
through an antiluteinizing effect mediated Endometrial Carcinoma
via the pituitary. May increase appetite by PO: ADULTS, ELDERLY: 40–320 mg/day
antagonizing metabolic effects of catabolic in divided doses for at least 2 mos.
cytokines. Therapeutic Effect: Reduces
tumor size. Increases appetite. Anorexia, Cachexia, Weight Loss
PO: ADULTS, ELDERLY: Initially, 625
mg
PHARMACOKINETICS (125 mg/mL suspension) or 800 mg (40
Well absorbed from GI tract. Metabo- mg/mL suspension) daily.
lized in liver. Excreted in urine. Half-
life: 13–105 hrs (mean 34 hrs). Dosage in Renal Impairment
Use caution.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: If possible, avoid Dosage in Hepatic Impairment
use during pregnancy, esp. first 4 mos. No dose adjustment.
Breastfeeding not recommended. Chil- SIDE EFFECTS
dren: Safety and efficacy not established.
Elderly: Use caution. Frequent: Weight gain secondary to
increased appetite. Occasional: Nau-
sea, breakthrough menstrual bleeding,

Canadian trade name Non-Crushable Drug High Alert drug


736 meloxicam

backache, headache, breast tenderness, PRECAUTIONS


carpal tunnel syndrome. Rare: Feeling Contraindications: Hypersensitivity to
of coldness. meloxicam. Pts with aspirin triad
(asthma, rhinitis, aspirin intoler-
ADVERSE EFFECTS/TOXIC ance). History of asthma, urticaria with
REACTIONS NSAIDs, perioperative pain in setting of
Thrombophlebitis, pulmonary embolism CABG surgery. Cautions: Renal/hepatic
occur rarely. impairment, asthma, coagulation disor-
ders, hypertension, history of GI disease
NURSING CONSIDERATIONS (bleeding or ulcers), concurrent use of
anticoagulants, fluid retention, HF, dehy-
BASELINE ASSESSMENT
dration, smoking, alcohol use, elderly,
Question for possibility of pregnancy. debilitated.
Provide support to pt, family, recognizing
that this drug is palliative, not curative. ACTION
INTERVENTION/EVALUATION Produces analgesic, antipyretic, anti-
Monitor for tumor response. Monitor pt inflammatory effects by inhibiting
weight, caloric intake (appetite stimulant). prostaglandin synthesis. Therapeutic
Effect: Reduces inflammatory response,
PATIENT/FAMILY TEACHING intensity of pain.
M • Contraception is imperative. • Re-
port lower leg (calf) pain, difficulty PHARMACOKINETICS
breathing, vaginal bleeding. • May Route Onset Peak Duration
cause headache, nausea, vomiting, PO (Analgesic) 30 min 4–5 hrs N/A
breast tenderness, backache.
Well absorbed after PO administration.
Protein binding: 99%. Metabolized in liver.
Excreted equally in urine, feces. Not removed
meloxicam by hemodialysis. Half-life: 15–20 hrs.
mel-ox-i-kam LIFESPAN CONSIDERATIONS
(Mobic, Qmiiz, Vivlodex) Pregnancy/Lactation: Avoid use at 30
j BLACK BOX ALERT jIncreased wks gestation or more (may cause prema-
risk of serious cardiovascular
thrombotic events, including myo- ture closure of ductus arteriosus). Dis-
cardial infarction, CVA. Increased tributed in breast milk. Children: Safety
risk of severe GI reactions, including and efficacy not established in children
ulceration, bleeding, GI perforation. younger than 2 yrs. Elderly: Age-related
renal impairment may require dosage
uCLASSIFICATION adjustment. More susceptible to GI toxic-
PHARMACOTHERAPEUTIC: NSAID. ity; lower dosage recommended.
CLINICAL: Anti-inflammatory, anal-
gesic. INTERACTIONS
DRUG: May increase anticoagulant effect of
apixaban, dabigatran, edoxaban, riva-
USES roxaban. Bile acid sequestrants (e.g.,
Relief of signs/symptoms of osteo- cholestyramine) may decrease absorption.
arthritis, rheumatoid arthritis (RA). May increase nephrotoxic effect of cycloSPO-
Treatment of juvenile idiopathic arthri- RINE, tacrolimus, tenofovir. May decrease
tis (JIA) in pts 2 yrs of age and older effect of loop diuretics (e.g., furose-
(suspension) and weighing 60 kg or mide). HERBAL: Glucosamine, herbals
more (tablets).
underlined – top prescribed drug
melphalan 737
with anticoagulant/antiplatelet proper- than 2%): Drowsiness, urticaria, photo-
ties (e.g., garlic, ginger, ginkgo biloba, sensitivity, tinnitus.
ginseng) may increase concentration/effect.
FOOD: None known. LAB VALUES: May ADVERSE EFFECTS/TOXIC
increase serum creatinine, ALT, AST. REACTIONS
In pts treated chronically, peptic ulcer, GI
AVAILABILITY (Rx) bleeding, gastritis, severe hepatic toxicity
Oral Suspension: (Mobic): 7.5 mg/5 mL. (jaundice), nephrotoxicity (hematuria,
Tablets: (Mobic): 7.5 mg, 15 mg. Cap- dysuria, proteinuria), severe hypersen-
sules: (Vivlodex): 5 mg, 10 mg. Tablet sitivity reaction (bronchospasm, angio-
ODT: (Qmiiz): 7.5 mg, 15 mg. edema) occur rarely.
ADMINISTRATION/HANDLING NURSING CONSIDERATIONS
PO BASELINE ASSESSMENT
• Give with food or milk to minimize GI
irritation. • Shake oral suspension gently Assess onset, type, location, duration of
before administering. • ODT: Do not re- pain/inflammation. Inspect appearance
move from blister until ready to administer. of affected joints for immobility, deformi-
Using dry hands, peel backing off the blis- ties, skin condition. Question history of
ter; do not push tablet through foil. Remove GI bleeding, gastric or duodenal ulcers,
tablet and place in mouth or on tongue and hepatic/renal impairment, asthma.
allow to disintegrate. Swallow with saliva INTERVENTION/EVALUATION M
(with or without drinking liquid). Monitor CBC, BMP, LFT. Assess skin for pe-
INDICATIONS/ROUTES/DOSAGE techiae. Assess for therapeutic response:
relief of pain, stiffness, swelling; increased
Osteoarthritis, Rheumatoid Arthritis (RA) joint mobility; reduced joint tenderness;
PO: (Mobic): ADULTS, ELDERLY: Ini- improved grip strength. Monitor for ab-
tially, 7.5 mg/day. Maximum: 15 mg/ dominal pain, hematemesis.
day (7.5 mg for pts on dialysis).
PATIENT/FAMILY TEACHING
Osteoarthritis • Take with food, milk to reduce GI up-
PO: (Vivlodex): ADULTS, ELDERLY: Ini- set. • Report tinnitus, persistent abdominal
tially, 5 mg once daily. May increase to 10 pain/cramping, severe nausea, vomiting, dif-
mg once daily. ficulty breathing, unusual bruising or bleed-
JIA
ing, rash, peripheral edema, chest pain, pal-
PO: (Suspension): CHILDREN, 2 YRS AND
pitations. • Avoid use after 30 wks gestation.
OLDER: 0.125 mg/kg once daily. Maxi-
mum: 7.5 mg. (Tablets): CHILDREN
WEIGHING 60 KG OR MORE: 7.5 mg once daily. melphalan
Dosage in Renal Impairment
mel-fa-lan
Not recommended with severe impairment. (Alkeran, Evomela)
Dosage in Hepatic Impairment j BLACK BOX ALERT jMyelo-
No dose adjustment. suppression is common. Potentially
mutagenic, leukemogenic. Hyper-
sensitivity noted with IV adminis-
SIDE EFFECTS tration. Must be administered by
Frequent (9%–7%): Dyspepsia, headache, certified chemotherapy personnel.
diarrhea, nausea. Occasional (4%–3%): Do not confuse Alkeran with Leu-
Dizziness, insomnia, rash, pruritus, flatu- keran or Myleran, or melphalan
lence, constipation, vomiting. Rare (less with Mephyton or Myleran.
Canadian trade name Non-Crushable Drug High Alert drug
738 melphalan
uCLASSIFICATION INTERACTIONS
PHARMACOTHERAPEUTIC: Alkylat- DRUG: Bone marrow depressants
ing agent. CLINICAL: Antineoplastic. (e.g., cladribine) may increase myelo-
suppression. May decrease the thera-
peutic effect of BCG (intravesical),
USES vaccines (live). May increase adverse
Treatment of nonresectable epithelial ovar- effects of natalizumab, vaccines (live).
ian carcinoma. Palliative treatment of mul- HERBAL: Echinacea may decrease
tiple myeloma or high-dose conditioning effects. FOOD: None known. LAB VAL-
treatment before hematopoietic stem cell UES: May increase serum uric acid.
transplantation (HSCT). OFF-LABEL: Hodg-
kin’s lymphoma, malignant melanoma, AVAILABILITY (Rx)
neuroblastoma, induction regimen for Injection, Powder for Reconstitution: 50
bone marrow and stem cell transplantation, mg. Tablets: (Alkeran): 2 mg.
light chain amyloidosis, Ewing’s sarcoma.
ADMINISTRATION/HANDLING
PRECAUTIONS
IV
Contraindications: Hypersensitivity to
melphalan (Alkeran). Resistance to prior Reconstitution • Reconstitute 50-mg
melphalan therapy. Cautions: Preexisting vial with diluent supplied by manufac-
bone marrow suppression, renal impair- turer to yield 5 mg/mL solution. • Fur-
M ment, pregnancy, prior chemotherapy or ther dilute with 0.9% NaCl to final con-
irradiation. centration not exceeding 0.45 mg/mL.
Rate of administration • Infuse
ACTION over 15–30 min at rate not to exceed 10
Inhibits DNA and RNA synthesis via mg/min (total infusion should be admin-
carbonium ion formation, cross-links istered within 1 hr).
strands of DNA, acts on resting and rap- Storage • Store at room temperature;
idly dividing tumor cells. Therapeutic protect from light. • Once reconsti-
Effect: Disrupts nucleic acid function, tuted, complete administration within
producing tumor cell death. 60 min.
PHARMACOKINETICS PO
Oral administration is highly variable. • Store tablets in refrigerator; protect
Incomplete intestinal absorption, variable from light. • Give on empty stomach (1
first-pass metabolism, rapid hydrolysis hr before or 2 hrs after meals).
may result. Protein binding: 60%–90%.
Extensively metabolized in blood. Elimi-
IV INCOMPATIBILITIES
nated from plasma primarily by chemi- Amphotericin B complex (Abelcet, AmBi-
cal hydrolysis. Partially excreted in feces; some, Amphotec).
minimal elimination in urine. Half-
life: PO: 1–1.25 hrs. IV: 1.5 hrs.
IV COMPATIBILITIES
Acyclovir, dexamethasone (Decadron),
LIFESPAN CONSIDERATIONS famotidine (Pepcid), furosemide (Lasix),
Pregnancy/Lactation: May cause fetal LORazepam (Ativan), morphine.
harm. Unknown if distributed in breast
milk. Children: Safety and efficacy
INDICATIONS/ROUTES/DOSAGE
not established. Elderly: Age-related b ALERT c WBC less than 3,000
renal impairment may require dosage cells/mm3, platelets less than
adjustment. 100,000 cells/mm3: Withhold treat-
ment until recovery.

underlined – top prescribed drug


memantine 739
Ovarian Carcinoma discontinuing drug. Hyperuricemia noted
PO: ADULTS, ELDERLY: 0.2 mg/kg/day by hematuria, crystalluria, flank pain.
for 5 successive days. Repeat at 4- to
5-wk intervals. NURSING CONSIDERATIONS
Multiple Myeloma (Palliative Treatment) BASELINE ASSESSMENT
PO: ADULTS: Initially, 6 mg once daily Obtain CBC, then wkly thereafter. Dosage
for 2–3 wks, followed by up to 4 wks rest, may be decreased or discontinued if WBC
then maintenance dose of 2 mg daily as falls below 3,000 cells/mm3 or platelet
hematologic recovery begins or 10 mg count falls below 100,000 cells/mm3. An-
daily for 7–10 days, then maintenance tiemetics may be effective in preventing/
dose of 2 mg daily (after WBC greater than treating nausea, vomiting.
4,000 cell/mm3 and platelets greater than INTERVENTION/EVALUATION
100,000 cells/mm3 titrated to hematologic
response or 0.15 mg/kg/day for 7 days Monitor CBC with differential, serum elec-
with 2–6 wks rest, then maintenance dose trolytes. Monitor for stomatitis. Monitor
of 0.05 mg/kg/day or 0.25 mg/kg/day for for hematologic toxicity (fever, sore throat,
4 days, then repeated at 4- to 6-wk inter- signs of local infection, unusual bruising/
vals as ANC and platelets return to normal. bleeding from any site), symptoms of ane-
IV: ADULTS: 16 mg/m2/dose every 2 wks mia (excessive fatigue, weakness), signs
for 4 doses, then repeat monthly after of hyperuricemia (hematuria, flank pain).
hematologic recovery. Avoid IM injections, rectal temperatures,
other traumas that may induce bleeding. M
Multiple Myeloma (Conditioning
before HSCT) PATIENT/FAMILY TEACHING
IV: ADULTS, ELDERLY: (Evomela only): • Increase fluid intake (may protect
100 mg/m2 daily for 2 days on day 3 and against hyperuricemia). • Maintain strict
2 before autologous stem cell transplant oral hygiene. • Hair loss is reversible, but
on day 0. new hair growth may have different color,
texture. • Avoid crowds, those with infec-
Dosage in Renal Impairment tions. • Report fever, shortness of breath,
IV: BUN LEVEL GREATER THAN 30 MG/ cough, sore throat, bleeding, unusual
DL: Decrease dosage by 50%. bruising. • May suppress ovarian func-
Dosage in Hepatic Impairment tion, leading to amenorrhea.
No dose adjustment.
SIDE EFFECTS memantine
Frequent: Nausea, vomiting (may be severe
with large dose). Occasional: Diarrhea, me-man-teen
stomatitis, rash, pruritus, alopecia. (Ebixa , Namenda, Namenda XR)

ADVERSE EFFECTS/TOXIC FIXED-COMBINATION(S)


REACTIONS Namzaric: memantine/donepezil (a
Myelosuppression manifested as hema- cholinesterase inhibitor): 7 mg/10
tologic toxicity (principally leukopenia, mg; 14 mg/10 mg; 21 mg/10 mg; 28
thrombocytopenia, and, to lesser extent, mg/10 mg.
anemia, pancytopenia, agranulocyto-
uCLASSIFICATION
sis). Leukopenia may occur as early as
5 days after drug initiation. WBC, platelet PHARMACOTHERAPEUTIC: NMDA
counts return to normal during 5th wk receptor antagonist. CLINICAL: Anti-
after therapy, but leukopenia, thrombo- Alzheimer’s agent.
cytopenia may last more than 6 wks after
Canadian trade name Non-Crushable Drug High Alert drug
740 memantine

USES Capsules, Extended-Release: (Na-


Treatment of moderate to severe dementia menda XR): 7 mg, 14 mg, 21 mg, 28 mg.
of Alzheimer’s type. OFF-LABEL: Treatment
of mild to moderate vascular dementia. ADMINISTRATION/HANDLING
PO
PRECAUTIONS • Give without regard to food. • Admin-
Contraindications: Hypersensitivity to ister oral solution using syringe provided.
memantine. Cautions: Moderate to Do not dilute or mix with other fluids.
severe renal impairment, severe hepatic • Give extended-release capsules whole.
impairment, cardiovascular disease, Do not crush. May open capsule and sprin-
seizure disorder, GU conditions that kle on applesauce; give immediately.
raise urine pH level.
INDICATIONS/ROUTES/DOSAGE
ACTION Alzheimer’s Disease
Decreases effects of glutamate, the prin- PO: ADULTS, ELDERLY: (Immediate-
cipal excitatory neurotransmitter in the Release): Initially, 5 mg once daily. May
brain. Persistent CNS excitation by glu- increase dosage at intervals of at least 1 wk
tamate is thought to cause symptoms in 5-mg increments to 10 mg/day (5 mg
of Alzheimer’s disease. Therapeutic twice daily), then 15 mg/day (5 mg and 10
Effect: May slow clinical deteriora- mg as separate doses), and finally 20 mg/
tion in moderate to severe Alzheimer’s day (10 mg twice daily). Target dose: 20
M disease. mg/day. (Extended-Release): Initially,
7 mg once daily. May increase at intervals
PHARMACOKINETICS of at least 7 days in increments of 7 mg.
Rapidly, completely absorbed after PO Maximum: 28 mg once daily. Switch-
administration. Protein binding: 45%. ing from immediate-release to extended-
Undergoes little metabolism; most of release: Begin the day following last dose
dose is excreted unchanged in urine. of immediate-release.
Half-life: 60–80 hrs. 10 mg twice daily: 28 mg once daily.
5 mg twice daily: 14 mg once daily.
LIFESPAN CONSIDERATIONS
Dosage in Renal Impairment
Pregnancy/Lactation: Unknown if
drug crosses placenta or is distrib- Dosage
uted in breast milk. Children: Not Creatinine Immediate- Extended-
prescribed for this pt population. Clearance Release Release
Elderly: No age-related precautions 30 mL/min or No adjust- No adjust-
noted, but use is not recommended in greater ments ments
5–29 mL/min 5 mg twice 14 mg once
pts with severe renal impairment (CrCl
daily or 10 daily
less than 9 mL/min). mg once
daily
INTERACTIONS
DRUG: Urine alkalinizers (e.g., car-
bonic anhydrase inhibitors, sodium Dosage in Hepatic Impairment
bicarbonate) may decrease renal Mild to moderate impairment: No
elimination. HERBAL: None significant. dose adjustment. Severe impairment:
FOOD: None known. LAB VALUES: None Use caution.
significant.
SIDE EFFECTS
AVAILABILITY (Rx) Occasional (7%–4%): Dizziness, headache,
Oral Solution: 10 mg/5 mL. Tablets: 5 mg, confusion, constipation, hypertension,
10 mg. cough. Rare (3%–2%): Back pain, nausea,

underlined – top prescribed drug


meropenem 741
fatigue, anxiety, peripheral edema, arthral- older; intra-abdominal infections; com-
gia, insomnia. plicated skin/skin structure infections
caused by susceptible S. aureus, S. pyo-
ADVERSE EFFECTS/TOXIC genes, S. agalactiae, S. pneumoniae,
REACTIONS H. influenzae, N. meningitidis, M.
None known. catarrhalis, E. coli, Klebsiella, Entero-
bacter, Serratia, P. aeruginosa, B. fra-
NURSING CONSIDERATIONS gilis. OFF-LABEL: Febrile neutropenia,
BASELINE ASSESSMENT liver abscess, otitis external, prosthetic
joint infection.
Assess cognitive, behavioral, functional
deficits of pt. Assess renal function. Ques- PRECAUTIONS
tion history of cardiovascular disease, he- Contraindications: Hypersensitivity to
patic/renal impairment, seizure disorder. me­ropenem, pts who experienced
INTERVENTION/EVALUATION anaphylactic reactions to other beta-
Monitor cognitive, behavioral, functional lactams. Cautions: Renal impairment,
status of pt. Monitor urine pH (altera- CNS disorders (particularly with history
tions of urine pH toward the alkaline of seizures, concurrent use with valproic
condition may lead to accumulation of acid).
the drug with possible increase in side ACTION
effects). Monitor BUN, CrCl, serum cre-
atinine lab values. Binds to penicillin-binding proteins. M
Inhibits bacterial cell wall synthesis.
PATIENT/FAMILY TEACHING Therapeutic Effect: Bactericidal.
• Do not reduce or stop medication; do
not increase dosage without physician PHARMACOKINETICS
direction. • Ensure adequate fluid in- After IV administration, widely distrib-
take. • If therapy is interrupted for sev- uted into tissues and body fluids, includ-
eral days, restart at lowest dose, titrate to ing CSF. Protein binding: 2%. Primarily
current dose at minimum of 1-wk inter- excreted unchanged in urine. Removed
vals. • Local chapter of Alzheimer’s by hemodialysis. Half-life: 1 hr.
Disease Association can provide a guide
to services. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if
distributed in breast milk. Children:
meropenem Safety and efficacy not established in
pts younger than 3 mos. Elderly: Age-
mer-oh-pen-em related renal impairment may require
(Merrem) dosage adjustment.
Do not confuse meropenem
with doripenem, ertapenem, or INTERACTIONS
imipenem. DRUG: May decrease effects of val-
proic acid. HERBAL: None significant.
uCLASSIFICATION FOOD: None known. LAB VALUES: May
PHARMACOTHERAPEUTIC: Carbap- increase serum BUN, alkaline phos-
enem. CLINICAL: Antibiotic. phatase, LDH, ALT, AST, bilirubin. May
decrease Hgb, Hct, WBC.

USES AVAILABILITY (Rx)


Treatment of multidrug-resistant infec- Injection, Powder for Reconstitution: 500
tions; meningitis in children 3 mos and mg, 1 g.

Canadian trade name Non-Crushable Drug High Alert drug


742 meropenem

ADMINISTRATION/HANDLING Dosage in Renal Impairment


Dosage and frequency are modified
IV based on creatinine clearance.
Reconstitution • Reconstitute each
500 mg with 10 mL Sterile Water for In- Creatinine
jection, 0.9% NaCl, or D5W to provide Clearance Dosage Interval
concentration of 50 mg/mL. • Shake to 26–49 mL/min Normal dose q12h
dissolve until clear. • May further dilute 10–25 mL/min 50% of normal q12h
with 0.9% NaCl or D5W to a concentra- dose
tion of 1–20 mg/mL. Less than 10 50% of normal q24h
Rate of administration • May give by mL/min dose
IV push or IV intermittent infusion (pig- Hemodialysis: 500 mg q24h
Peritoneal Recommended q24h
gyback). • If administering as IV inter- ­dialysis: dose (based
mittent infusion (piggyback), give over on indication)
15–30 min (may also give over 3 hrs); if
administered by IV push, give over 3–5 Continuous Renal Replacement Therapy
min (at a concentration not greater than (CRRT)
Dosage Interval
50 mg/mL).
Continuous 1 gram then q8h OR
Storage • Store vials at room temper-
­venovenous 500 mg OR 1 q12h
ature. • After reconstitution of vials hemofiltration gram
with 0.9% NaCl, stable for 2 hrs at room Continuous 1 gram then q6–8h OR
M temperature or 18 hrs if refrigerated venovenous 500 mg OR 1 q8–12h
(with D5W, stable for 1 hr at room tem- hemodialysis/ gram
perature, 8 hrs if refrigerated). IV infu- continuous
sion with 0.9% NaCl stable for 4 hrs at venovenous
room temperature or 24 hrs if refriger- hemodia­
filtration
ated (with D5W, 1 hr at room tempera-
ture or 4 hrs if refrigerated).
Dosage in Hepatic Impairment
IV INCOMPATIBILITIES No dose adjustment.
Acyclovir (Zovirax), amphotericin B (Fun-
gizone), diazepam (Valium), doxycycline SIDE EFFECTS
(Vibramycin), metroNIDAZOLE (Flagyl), Frequent (5%–3%): Diarrhea, nausea,
ondansetron (Zofran). vomiting, headache, inflammation at
injection site. Occasional (2%): Oral can-
IV COMPATIBILITIES didiasis, rash, pruritus. Rare (less than
Dexamethasone (Decadron), DOBUTa- 2%): Constipation, glossitis.
mine (Dobutrex), DOPamine (Intropin),
furosemide (Lasix), heparin, magnesium, ADVERSE EFFECTS/TOXIC
morphine. REACTIONS
Antibiotic-associated colitis, other superin-
INDICATIONS/ROUTES/DOSAGE fections (abdominal cramps, severe watery
Usual Dosage diarrhea, fever) may result from altered
IV: ADULTS, ELDERLY: 500 mg q6h or bacterial balance in GI tract. Anaphylactic
1–2g q8h. (Extended-Infusion): 1–2 reactions have been reported. Seizures may
g over 3 hrs q8h. CHILDREN, ADOLES- occur in pts with CNS disorders (e.g., brain
CENTS: 20 mg/kg/dose q8h. Maximum lesions, history of seizures), bacterial men-
dose: 1,000 mg. NEONATES: 20 mg/kg/ ingitis, renal impairment.
dose q8–12h.

underlined – top prescribed drug


meropenem/vaborbactam 743

PRECAUTIONS
NURSING CONSIDERATIONS
Contraindications: Known hypersensi-
BASELINE ASSESSMENT tivity to meropenem, cephalosporins,
Question history of hypersensitivity, penicillin; anaphylaxis to beta-lactams.
allergic reaction to penicillins, cepha- Cautions: History of renal impairment,
losporins. Inquire about history of sei- seizure disorder, recent Clostridium
zures. difficile infection or antibiotic-asso-
ciated colitis; prior hypersensitivity to
INTERVENTION/EVALUATION carbapenem, PCN.
Monitor daily pattern of bowel activity,
stool consistency. Monitor for nausea, ACTION
vomiting. Evaluate for inflammation at IV Meropenem binds to penicillin-
injection site. Assess skin for rash. Evalu- binding proteins, inhibiting cell wall
ate hydration status. Monitor I&O, renal synthesis. Vaborbactam protects
function, LFT. Check mental status; be meropenem from serine beta-lacta-
alert to tremors, possible seizures. Assess mase degradation (vaborbactam has
temperature, B/P twice daily, more often no antibacterial activity). Therapeutic
if necessary. Monitor serum electrolytes, Effect: Bactericidal.
esp. potassium.
PHARMACOKINETICS
PATIENT/FAMILY TEACHING
Widely distributed into tissues and
• Report persistent diarrhea, abdominal body fluids. Meropenem metabolized M
cramps, fever. by hydrolysis. Vaborbactam does not
undergo metabolism. Protein binding:
(meropenem): less than 2%; (vabor-
bactam): 33%. Excreted unchanged in
meropenem/ urine. Half-life: 1–2 hrs.
vaborbactam LIFESPAN CONSIDERATIONS
mer-oh-pen-em/va-bor-bak-tam Pregnancy/Lactation: Meropenem
(Vabomere) is secreted in break milk. Unknown if
Do not confuse meropenem/ vaborbactam is distributed in breast
vaborbactam with ampicillin/ milk. Children: Safety and efficacy
sulbactam, certolozane/tazobac- not established. Elderly: May have
tam, ceftazidime/avibactam, or increased risk of adverse effects in pts
piperacillin/tazobactam. with renal impairment.

uCLASSIFICATION INTERACTIONS
PHARMACOTHERAPEUTIC: Carbape- DRUG: Probenecid may increase con-
nem/beta-lactamase inhibitor. CLINI- centration/effect of meropenem. May
CAL: Antibacterial. decrease concentration/effect of val-
proic acid, divalproex. May decrease
effect of BCG (intravesical). HERBAL:
USES None significant. FOOD: None known.
Treatment of pts 18 yrs and older with LAB VALUES: May increase serum ALT,
complicated urinary tract infections AST. May decrease eosinophils, leuko-
(UTIs), including pyelonephritis, caused cytes, lymphocytes; serum potassium.
by the following susceptible microorgan- May result in positive Coombs’ test.
isms: E. coli, K. pneumoniae, Entero- May decrease platelets in pts with renal
bacter cloacae species. impairment.

Canadian trade name Non-Crushable Drug High Alert drug


744 meropenem/vaborbactam

AVAILABILITY (Rx) Dosage in Renal Impairment


b ALERT c Meropenem/vaborbactam is Note: Infuse after hemodialysis on
a combination product. hemodialysis days. Dosage is modified
Injection, Powder for Reconstitution:
based on eGFR.
meropenem/vaborbactam: 1 g/1 g. Estimated Glomerular
Filtration Rate Dosage
ADMINISTRATION/HANDLING
eGFR 30–49 mL/min 2 g q8h
IV eGFR 15–29 mL/min 2 g q12h
Reconstitution • Calculate the num- eGFR less than 15 mL/min 1 g q12h
ber of vials needed for dose. • Reconsti-
tute each vial with 20 mL 0.9% NaCl Dosage in Hepatic Impairment
(withdrawn from infusion bag) to a final Mild to severe impairment: No dose
concentration of 0.05 g/mL of meropenem adjustment.
and 0.05 g/mL of vaborbactam. • Final
volume of vial equals 21.3 mL. • Gently SIDE EFFECTS
mix until powder is fully dissolved. • Vi- Occasional (9%–4%): Headache, infu-
sually inspect for particulate matter or sion site reactions (phlebitis, erythema,
discoloration. Solution should appear col- thrombosis). Rare (3%–2%): Diarrhea,
orless to slightly yellow in color. pyrexia.
Dilution • 4-g dose (2 vials): Dilute
M volume of each vial (21 mL/vial) in 0.9% ADVERSE EFFECTS/TOXIC
NaCl bag with a volume of 250 mL (16 mg/ REACTIONS
mL), or 500 mL (8 mg/mL), or 1,000 mL Hypersensitivity reactions, including
(4 mg/mL). • 2-g dose (1 vial): Dilute anaphylaxis, have been reported in pts
the volume of vial (21 mL) in 0.9% NaCl treated with beta-lactam antibacterial
bag with a volume of 125 mL (16 mg/mL), drugs. Blood and lymphatic disorders
or 250 mL (8 mg/mL), or 500 mL (4 mg/ such as agranulocytosis, hemolytic
mL). • 1-g dose (1 vial): Dilute half of anemia, leukopenia, lymphocytosis,
the volume of vial (10.5 mL) in 0.9% NaCl neutropenia, thrombocytopenia were
bag with volume of 70 mL (14.3 mg/mL), or reported. Seizures may occur in pts
125 mL (8 mg/mL), or 250 mL (4 mg/mL). with CNS disorders (e.g., brain lesion,
Rate of administration • Infuse over history of seizures, bacterial meningi-
3 hrs. tis), renal impairment. Other CNS reac-
Storage • Refrigerate diluted solution tions may include tremor, paresthesia,
for up to 22 hrs or store at room tempera- lethargy. Clostridium difficile–asso-
ture for up to 4 hrs. • Diluted solution ciated diarrhea, with severity ranging
must be completely infused within 4 hrs. from mild diarrhea to fatal colitis, was
reported. Clostridium difficile infec-
IV INCOMPATIBILITIES tion may occur more than 2 mos after
Acyclovir (Zovirax), amphotericin B (Fun- completion of treatment. May increase
gizone), diazepam (Valium), doxycycline risk of development of drug-resistant
(Vibramycin), metronidazole (Flagyl), on- bacteria when used in the absence of a
dansetron (Zofran). proven or strongly suspected bacterial
infection. Skin and SQ reactions includ-
INDICATIONS/ROUTES/DOSAGE ing angioedema, erythema multiforme,
Complicated Urinary Tract Infections pruritus, Stevens-Johnson syndrome,
Including Pyelonephritis toxic epidermal necrolysis occur rarely.
IV: ADULTS, ELDERLY: 4 g (meropenem Secondary infections including pharyn-
2 g/vaborbactam 2 g) q8h for up to 14 gitis, oral or vulvovaginal candidiasis
days. may occur.

underlined – top prescribed drug


mesalamine 745

NURSING CONSIDERATIONS changes such as anxiety, confusion, hal-


lucinations, muscle jerking, or seizure-
BASELINE ASSESSMENT like activity. • Severe allergic reactions
Obtain BUN, serum creatinine, CrCl, such as hives, palpitations, shortness of
GFR in pt with renal impairment. Obtain breath, rash, tongue swelling may occur.
urine culture and sensitivity. Question
history of renal impairment, seizure
disorder, recent C. diff infection; hy-
persensitivity reaction to beta-lactams, mesalamine
cephalosporins, PCN. Question pt’s
usual stool characteristics (color, fre- me-sal-a-meen
quency, consistency). (Apriso, Asacol HD, Canasa, Del-
zicol, Lialda, Mesasal , Pentasa,
INTERVENTION/EVALUATION Rowasa, Salofalk , sfRowasa)
Periodically monitor WBC. Monitor BUN, Do not confuse Asacol with
serum creatinine, CrCl, GFR, platelet Os-Cal, Lialda with Aldara, or
count in pts with renal impairment. Ob- mesalamine with megestrol,
serve daily pattern of bowel activity, stool memantine, or methenamine.
consistency (increased severity may in- uCLASSIFICATION
dicate antibiotic-associated colitis). If
frequent diarrhea occurs, obtain Clos- PHARMACOTHERAPEUTIC: Sali-
cylic acid derivative. CLINICAL: Anti- M
tridium difficile toxin screen and initi-
ate isolation precautions until test result inflammatory agent.
confirmed; manage proper fluid levels/
PO intake, electrolyte levels, protein USES
intake. Antibacterial drugs that are not
directed against Clostridium difficile PO: Treatment, maintenance of remis-
infection may need to be discontinued. sion of mild to moderate active ulcer-
Report any signs of hypersensitivity reac- ative colitis. Rectal: Treatment of active
tion. Assess skin for toxic skin reactions. mild to moderate distal ulcerative coli-
Monitor for seizure activity, CNS reac- tis, proctosigmoiditis or proctitis. OFF-
LABEL: Crohn’s disease.
tions, IV site reactions.
PATIENT/FAMILY TEACHING
PRECAUTIONS
• It is essential to complete drug ther- Contraindications: Hypersensitivity to
apy despite symptom improvement. Early mesalamine, salicylates. Cautions: Sul-
discontinuation may result in antibacte- fasalazine, active peptic ulcer, pyloric
rial resistance or may increase risk of stenosis, pericarditis, myocarditis, renal/
recurrent infection. • Report any epi- hepatic impairment, elderly.
sodes of diarrhea, esp. the following ACTION
months after last dose. Frequent loose
stool, fever, abdominal pain, blood- Mechanism unknown. May modulate
streaked stool may indicate infectious local mediators of inflammation, may
diarrhea and may be contagious to oth- inhibit tumor necrosis factor. Thera-
ers. • Report abdominal pain, black/ peutic Effect: Diminishes inflamma-
tarry stools, bruising, yellowing of skin tion in colon.
or eyes; dark urine, decreased urine PHARMACOKINETICS
output; skin problems such as develop-
ment of sores, rash, skin bubbling/ne- Poorly absorbed from colon. Moderately
crosis. • Report any nervous system absorbed from GI tract. Metabolized in
liver. Unabsorbed portion excreted in
Canadian trade name Non-Crushable Drug High Alert drug
746 mesalamine
feces; absorbed portion excreted in urine. INDICATIONS/ROUTES/DOSAGE
Unknown if removed by hemodialysis. Half- Treatment of Ulcerative Colitis
life: 0.5–1.5 hrs; metabolite, 5–10 hrs. PO: (Capsule [Pentasa]): ADULTS,
ELDERLY: 1 g 4 times daily.
LIFESPAN CONSIDERATIONS
PO: (Capsule [Delzicol]): ADULTS,
Pregnancy/Lactation: Unknown if drug ELDERLY: 800 mg 3 times daily. CHILDREN 5
crosses placenta or is distributed in breast YRS AND OLDER, WEIGHING 54–90 KG: 1,200
milk. Children: Safety and efficacy not mg in morning and evening. Maxi-
established. Elderly: Age-related renal mum: 2,400 mg/day. 33–53 KG: 1,200 mg
impairment may require dosage adjustment. in morning and 800 mg in evening. Maxi-
mum: 2,000 mg/day. 17–32 KG: 800 mg
INTERACTIONS
in morning and 400 mg in evening. Maxi-
DRUG: Antacids, histamine H2-recep- mum: 1,200 mg/day.
tor antagonists (e.g., famotidine, PO: (Tablet [Asacol HD]): ADULTS,
ranitidine), proton pump inhibi- ELDERLY: 1.6 g 3 times daily.
tors (e.g., lansoprazole, pantopra- PO: (Tablet [Lialda]): ADULTS, ELDERLY:
zole) may decrease therapeutic effect. 2.4–4.8 g once daily.
HERBAL: None significant. FOOD: None
known. LAB VALUES: May increase serum Maintenance of Remission in Ulcerative
alkaline phosphatase, ALT, AST, bilirubin. Colitis
PO: (Capsule [Pentasa]): ADULTS, ELD­
M AVAILABILITY (Rx) ERLY: 1 g 4 times daily.
Rectal Suspension: (Rowasa, sfRowasa): 4 PO: (Capsule [Delzicol]): ADULTS, ELD­
g/60 mL. Suppositories: (Canasa): 1 g. ERLY: 1.6 g/day in 2–4 divided doses.
Capsules, Controlled-Release: (Pen- PO: (Capsule, Extended-Release [Apr­
tasa): 250 mg, 500 mg. Extended-Release: iso]): ADULTS, ELDERLY: 1.5 g once daily in
(Apri­so): 375 mg. Capsules, Delayed- the morning.
Release: (Delzicol): 400 mg. Tablets, PO: (Tablet [Lialda]): 2.4 g once daily
Delayed-Release: (Asacol HD): 800 mg. with food.
(Lialda): 1.2 g.
Distal Ulcerative Colitis,
ADMINISTRATION/HANDLING Proctosigmoiditis, Proctitis
b ALERT c Store rectal suspension, sup- Rectal: (Retention Enema): ADULTS,
pository, oral forms at room temperature. ELDERLY: 60 mL (4 g) at bedtime; retained
overnight for approximately 8 hrs for 3–6
PO wks.
• Have pt swallow whole; do not break Rectal: (1 G Suppository): ADULTS,
outer coating of tablet. • Give without ELDERLY: Once daily at bedtime. Continue
regard to food. • Apriso: Do not ad- therapy for 3–6 wks.
minister with antacids. • Lialda: Ad- b ALERT c Suppository should be re-
minister once daily with meal. tained for 1–3 hrs for maximum benefit.

Rectal Dosage of Renal/Hepatic Impairment


• Shake bottle well. • Instruct pt to lie on Use caution.
left side with lower leg extended, upper leg
flexed forward. • Knee-chest position SIDE EFFECTS
may also be used. • Insert applicator tip Mesalamine is generally well tolerated,
into rectum, pointing toward umbili- with only mild, transient effects. Fre-
cus. • Squeeze bottle steadily until con- quent (greater than 6%): PO: Abdominal
tents are emptied. • Store suppositories cramps/pain, diarrhea, dizziness, head-
at room temperature. Do not refrigerate. ache, nausea, vomiting, rhinitis, unusual

underlined – top prescribed drug


mesna 747
fatigue. Rectal: Abdominal/stomach USES
cramps, flatulence, headache, nausea. Detoxifying agent used as protectant
Occasional (6%–2%): PO: Hair loss, against hemorrhagic cystitis induced
decreased appetite, back/joint pain, flat- by ifosfamide. OFF-LABEL: Reduce inci-
ulence, acne. Rectal: Alopecia. Rare dence of cyclophosphamide-induced
(less than 2%): Rectal: Anal irritation. hemorrhagic cystitis with high-dose
cyclophosphamide.
ADVERSE EFFECTS/TOXIC
REACTIONS PRECAUTIONS
Sulfite sensitivity may occur in susceptible Contraindications: Hypersensitivity to
pts, manifested as cramping, headache, mesna. Cautions: Preexisting autoim-
diarrhea, fever, rash, urticaria, pruritus, mune disorders.
wheezing. Discontinue drug immediately.
Hepatitis, pancreatitis, pericarditis occur ACTION
rarely with oral forms. Binds with, detoxifies urotoxic metabo-
lites of ifosfamide/cyclophosphamide.
NURSING CONSIDERATIONS
Therapeutic Effect: Inhibits ifosfamide/
BASELINE ASSESSMENT cyclophosphamide-induced hemorrhagic
Obtain BUN, serum creatinine, LFT. As- cystitis.
sess for abdominal pain, discomfort.
PHARMACOKINETICS
INTERVENTION/EVALUATION Rapidly metabolized after IV administra- M
Encourage adequate fluid intake. As- tion to mesna disulfide, which is reduced
sess bowel sounds for peristalsis. Moni- to mesna in kidneys. Protein binding:
tor daily pattern of bowel activity, stool 69%–75%. Excreted in urine. Half-life:
consistency; record time of evacuation. 24 min; metabolite: 72 min.
Assess for abdominal disturbances. As-
sess skin for rash, urticaria. Discontinue LIFESPAN CONSIDERATIONS
medication if rash, fever, cramping, or Pregnancy/Lactation: Unknown if
diarrhea occurs. drug crosses placenta or is distributed
in breast milk. Children: Safety and
PATIENT/FAMILY TEACHING
efficacy not established. Elderly: Infor-
• Report rash, fever, abdominal pain, mation not available.
significant diarrhea. • Avoid tasks that
require alertness, motor skills until re- INTERACTIONS
sponse to drug is established. • May DRUG: None significant. HERBAL: None
discolor urine yellow-brown. • Sup- significant. FOOD: None known. LAB
positories stain fabrics. VALUES: May produce false-positive test
result for urinary ketones.
AVAILABILITY (Rx)
mesna Injection Solution: 100 mg/mL. Tablets:
400 mg.
mess-na
(Mesnex, Uromitexan ) ADMINISTRATION/HANDLING
IV
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Chemo- Reconstitution • Dilute with D5W or
protective agent. CLINICAL: Antineo- 0.9% NaCl to concentration of 20 mg/
plastic adjunct, antidote. mL. • May add to solutions containing
ifosfamide or cyclophosphamide.
Canadian trade name Non-Crushable Drug High Alert drug
748 metFORMIN
Rate of administration • Administer ADVERSE EFFECTS/TOXIC
by IV infusion over 15–30 min or by REACTIONS
continuous infusion. Hematuria occurs rarely.
Storage • Store parenteral form at
room temperature. • After dilution, in NURSING CONSIDERATIONS
0.9% NaCl or D5W, stable for 48 hrs at
room temperature (solutions of mesna and BASELINE ASSESSMENT
cyclophosphamide in D5W stable for 48 hrs b ALERT c Each dose must be adminis-
if refrigerated or 6 hrs at room tempera- tered with ifosfamide therapy.
ture). Discard unused medication. INTERVENTION/EVALUATION
PO Assess morning urine specimen for he-
• Administer orally in either tablet for- maturia. If such occurs, dosage reduc-
mulation or parenteral solution. • Di- tion or discontinuation may be necessary.
lute mesna solution before PO adminis- Monitor daily pattern of bowel activity,
tration to decrease sulfur odor. Can be stool consistency; record time of evacua-
diluted (1:1 to 1:10) in carbonated cola tion. Monitor B/P for hypotension.
drinks, fruit juices, milk. PATIENT/FAMILY TEACHING
IV INCOMPATIBILITIES • Report headache, myalgia, nausea.
Amphotericin B complex (Abelcet, AmBi-
some, Amphotec), CISplatin (Platinol).
M
IV COMPATIBILITIES metFORMIN
Allopurinol (Aloprim), DOCEtaxel (Tax- met-for-min
otere), DOXOrubicin (Adriamycin), (Fortamet, Glucophage, Glucophage
etoposide (VePesid), gemcitabine (Gem- XR, Glumetza, Glycon , Riomet,
zar), granisetron (Kytril), methotrexate, D-Care DM2)
ondansetron (Zofran), PACLitaxel (Taxol),
vinorelbine (Navelbine). j BLACK BOX ALERT jLactic
acidosis occurs very rarely, but
mortality rate is 50%. Risk increases
INDICATIONS/ROUTES/DOSAGE with degree of renal impairment,
Prevention of Hemorrhagic Cystitis in Pts pt’s age, those with diabetes,
Receiving Ifosfamide unstable or acute HF.
IV: ADULTS, ELDERLY: 20% of ifosfamide Do not confuse Glucophage with
dose at time of ifosfamide administration Glucotrol, or metFORMIN with
and 4 and 8 hrs after each dose of ifos- metroNIDAZOLE.
famide. Total dose: 60% of ifosfamide FIXED-COMBINATION(S)
dosage.
IV/PO: 100% of ifosfamide dose, given Actoplus Met: metFORMIN/piogli-
as 20% IV at start time of ifosphamide, tazone (an antidiabetic): 500 mg/15
followed by 40% dose given orally 2 and mg, 850 mg/15 mg. Avandamet:
6 hrs after start of ifosfamide. metFORMIN/rosiglitazone (an anti-
diabetic): 500 mg/1 mg, 500 mg/2 mg,
Dosage in Renal/Hepatic Impairment 500 mg/4 mg, 1,000 mg/2 mg, 1,000
No dose adjustment. mg/4 mg. Glucovance: metFORMIN/
glyBURIDE (an antidiabetic): 250
SIDE EFFECTS mg/1.25 mg, 500 mg/2.5 mg, 500 mg/5
Frequent (greater than 17%):Altered taste, mg. Invokamet: metFORMIN/cana-
soft stools. Large doses: Diarrhea, myal- gliflozin (an antidiabetic): 500 mg/50
gia, headache, fatigue, nausea, hypoten- mg, 500 mg/150 mg, 1,000 mg/50 mg,
sion, allergic reaction. 1,000 mg/150 mg. Janumet, Janumet
underlined – top prescribed drug
metFORMIN 749
XR: metFORMIN/SITagliptin (an anti- alcohol intake, elderly. Recommend tem-
diabetic): 500 mg/50 mg, 1,000 mg/50 porary discontinuation at time of or before
mg. Jentadueto, Jentadueto XR: iodinated contrast imaging procedures in pts
metFORMIN/linagliptin (an antidia- with CrCl of 30–60 mL/min, or with history of
betic): 500 mg/2.5 mg; 1,000 mg/2.5 hepatic disease, alcoholism, HF.
mg; 1,000 mg extended-release/2.5
mg; 1,000 mg extended-release/5 ACTION
mg. Kazano: metFORMIN/alogliptin Decreases hepatic production of glu-
(an antidiabetic): 500 mg/12.5 mg; cose. Decreases intestinal absorption
1,000 mg/12.5 mg. Kombiglyze XR: of glucose, improves insulin sensitivity.
metFORMIN/SAXagliptin (an antidia- Therapeutic Effect: Improves glyce-
betic): 500 mg/5 mg, 1,000 mg/5 mg, mic control, stabilizes/decreases body
1,000 mg/2.5 mg. Metaglip: met- weight, improves lipid profile.
FORMIN/glipiZIDE (an antidiabetic):
250 mg/2.5 mg, 500 mg/2.5 mg, 500 PHARMACOKINETICS
mg/5 mg. Qternmet XR: metFORMIN/ Slowly, incompletely absorbed after PO
dapagliflozin (an antidiabetic)/saxa- administration. Food delays, decreases
gliptin (an antidiabetic): 1,000 mg/2.5 extent of absorption. Protein binding:
mg/2.5 mg; 1,000 mg/5 mg/2.5 mg; Negligible. Primarily distributed to intes-
1,000 mg/5 mg/5 mg; 1,000 mg/10 tinal mucosa, salivary glands. Primarily
mg/5 mg. PrandiMet: metFORMIN/ excreted unchanged in urine. Removed
repaglinide (an antidiabetic): 500 by hemodialysis. Half-life: 9–17 hrs. M
mg/1 mg, 500 mg/2 mg. Synjardy:
metFORMIN/empagliflozin (an antidia- LIFESPAN CONSIDERATIONS
betic): 500 mg/5 mg, 1,000 mg/5 mg, Pregnancy/Lactation: Insulin is drug
500 mg/12.5 mg, 1,000 mg/12.5 mg. of choice during pregnancy. Distributed in
breast milk in animals. Children: Safety
uCLASSIFICATION and efficacy not established in children
PHARMACOTHERAPEUTIC: Biguanide younger than 10 yrs. Elderly: Age-related
antihyperglycemic. CLINICAL: Anti- renal impairment or peripheral vascular
diabetic agent. disease may require dosage adjustment or
discontinuation.
USES INTERACTIONS
Management of type 2 diabetes mellitus. DRUG: Alcohol may increase adverse
OFF-LABEL: Polycystic ovarian syndrome, effects. Cimetidine, dolutegravir, rano-
gestational diabetes mellitus. Prevention lazine may increase concentration/effect.
of type 2 diabetes. IV contrast dye may increase risk of
metformin-induced lactic acidosis, acute
PRECAUTIONS renal failure (discontinue metFORMIN
b ALERT c Lactic acidosis is a rare but 24–48 hrs prior to and up to 72 hrs after
potentially severe consequence of met- contrast exposure). HERBAL: Garlic may
formin therapy. Withhold in pts with con- cause hypoglycemia. FOOD: None known.
ditions that may predispose to lactic aci- LAB VALUES: May alter cholesterol, LDL,
dosis (e.g., hypoxemia, dehydration, triglycerides, HDL.
hypoperfusion, sepsis).
Contraindications: Hypersensitivity to AVAILABILITY (Rx)
met­formin. Severe renal disease/dysfunc- Oral Solution: (Riomet): 100 mg/mL. Tab-
tion; acute or chronic metabolic acidosis lets: 500 mg, 850 mg, 1,000 mg.
(with or without coma). Cautions: HF, Tablets, Extended-Release: 500 mg,
hepatic impairment, excessive acute/chronic 750 mg, 1,000 mg.
Canadian trade name Non-Crushable Drug High Alert drug
750 metFORMIN

ADMINISTRATION/HANDLING during therapy. Rare (3%–1%): Unpleasant/


PO metallic taste that resolves spontaneously
• Give extended-release tablets whole. during therapy.
Do not break, crush, dissolve, or divide
ADVERSE EFFECTS/TOXIC
extended-release tablets. • Give with
REACTIONS
meals (to decrease GI upset). Give For-
tamet with glass of water. Lactic acidosis occurs rarely (0.03
cases/1,000 pts) but is a serious and
INDICATIONS/ROUTES/DOSAGE often fatal (50%) complication. Lactic
b ALERT c Allow 1–2 wks between acidosis is characterized by increase
dose titrations. in blood lactate levels (greater than 5
mmol/L), decrease in blood pH, elec-
Diabetes Mellitus trolyte disturbances. Symptoms include
PO: (Immediate-Release Tablets, Solu- unexplained hyperventilation, myalgia,
tion): ADULTS, ELDERLY: Initially, 500 mg malaise, drowsiness. May advance to car-
twice daily or 850 mg once daily. Titrate diovascular collapse (shock), acute HF,
in increments of 500 mg wkly or 850 mg acute MI, prerenal azotemia.
every other wk. May also titrate from 500
mg twice daily to 850 mg twice daily after NURSING CONSIDERATIONS
2 wks. Maintenance: 1,000–2,550 BASELINE ASSESSMENT
mg/day in 2–3 divided doses. Maxi-
M Verify pt has not received IV contrast dye
mum: 2,550 mg/day. CHILDREN 10–16
within last 48 hrs. Obtain CBC, renal func-
YRS: Initially, 500 mg twice daily. Main-
tion test, fasting serum glucose, Hgb A1c.
tenance: Titrate in 500-mg increments
wkly. Maximum: 2,000 mg/day. INTERVENTION/EVALUATION
PO: (Extended-Release Tablets): Monitor fasting serum glucose, Hgb A1c,
ADULTS, ELDERLY: Initially, 500–1,000 renal function, CBC. Monitor folic acid, re-
mg once daily. May increase by 500 mg nal function tests for evidence of early lactic
at 1-wk intervals. Maximum: 2,000 acidosis. If pt is on concurrent oral sulfo-
mg/day (Fortamet, Glucophage XR, nylureas, assess for hypoglycemia (cool/wet
Glumetza: 2,500 mg/day). skin, tremors, dizziness, anxiety, headache,
tachycardia, numbness in mouth, hunger,
Dosage in Renal Impairment
diplopia). Be alert to conditions that alter
Contraindicated in pts with serum creatinine
glucose requirements: fever, increased ac-
greater than 1.5 mg/dL (males) or greater
tivity, stress, surgical procedure. If lactic
than 1.4 mg/dL (females). Alternative
acidosis occurs, withhold treatment.
recommendation: CrCl 45–60 mL/
min: Continue use; monitor renal func- PATIENT/FAMILY TEACHING
tion q3–6 mos. CrCl 30–44 mL/min: Use • Report symptoms of lactic acidosis
caution. Consider dose reduction; monitor (unexplained hyperventilation, muscle
renal function q3mos. CrCL less than 30 aches, extreme fatigue, unusual drowsi-
mL/min: Discontinue use. ness). • Prescribed diet is principal
part of treatment; do not skip, delay
Dosage in Hepatic Impairment
meals. • Diabetes requires lifelong con-
Avoid use (risk factor for lactic acidosis).
trol. • Avoid alcohol. • Report persis-
SIDE EFFECTS tent headache, nausea, vomiting, diarrhea
or if skin rash, unusual bruising/bleeding,
Occasional (greater than 3%): GI dis-
change in color of urine or stool oc-
turbances (diarrhea, nausea, vomiting,
curs. • Do not take dose for at least 48
abdominal bloating, flatulence, anorexia)
hrs after receiving IV contrast dye with
that are transient and resolve spontaneously
radiologic testing.
underlined – top prescribed drug
methadone 751
hypothyroidism, Addison’s disease, head
methadone injury, increased intracranial pressure.
meth-a-done ACTION
(Dolophine, Metadol , Methadone Binds with opioid receptors within CNS,
Intensol, Methadose) causing inhibition of ascending pain path-
j BLACK BOX ALERT jMay pro- ways. Therapeutic Effect: Produces gen-
long QT interval, which may cause eralized CNS depression. Alters processes
serious arrhythmias. May cause
serious, life-threatening, or fatal affecting analgesia, emotional response to
respiratory depression. Monitor for pain; reduces withdrawal symptoms from
signs of misuse, abuse, addiction. other opioid drugs.
Prolonged maternal use may cause
neonatal withdrawal syndrome. PHARMACOKINETICS
Do not confuse methadone Route Onset Peak Duration
with Mephyton, Metadate CD,
PO 0.5–1 hr 1.5–2 hrs 6–8 hrs
Metadate ER, methylphenidate, IM 10–20 min 1–2 hrs 4–5 hrs
or morphine. IV N/A 15–30 min 3–4 hrs
uCLASSIFICATION Well absorbed after IM injection. Protein
PHARMACOTHERAPEUTIC: Opi- binding: 85%–90%. Metabolized in liver.
oid agonist (Schedule II). CLINI- Primarily excreted in urine. Not removed
CAL: Opioid analgesic. Opioid de- by hemodialysis. Half-life: 7–59 hrs. M
pendency management.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses pla-
USES centa. Distributed in breast milk. Respi-
Oral: Moderate to severe pain when a ratory depression may occur in neonate
continuous around-the-clock analgesic if mother received opiates during labor.
is needed. Detoxification/maintenance Regular use of opiates during pregnancy
treatment of opioid addiction in conjunc- may produce withdrawal symptoms in
tion with social/medical services. Injec- neonate (irritability, excessive crying,
tion: Management of pain severe enough tremors, hyperactive reflexes, fever, vomit-
to require an opioid analgesic when ing, diarrhea, yawning, sneezing, seizures).
alternate options are inadequate. Children: Paradoxical excitement may
occur. Pts younger than 2 yrs more sus-
PRECAUTIONS ceptible to respiratory depressant effects.
Contraindications: Hypersensitivity to Elderly: More susceptible to respira-
methadone. Severe respiratory depres- tory depressant effects. Age-related renal
sion, acute or severe bronchial asthma impairment may increase risk of urinary
(in absence of resuscitative equipment retention.
or unmonitored setting), hypercarbia,
GI obstruction including paralytic ileus INTERACTIONS
(known or suspected). Cautions: Renal/ DRUG: Alcohol, other CNS depres-
hepatic impairment, elderly/debilitated pts, sants (e.g., LORazepam, mor-
risk for QT prolongation, medications that phine, zolpidem) may increase
prolong QT interval, conduction abnor- CNS effects, respiratory depression,
malities, severe volume depletion, hypo- hypotension. Strong CYP3A4 induc-
kalemia, hypomagnesemia, cardiovascular ers (e.g., carBAMazepine, phe-
disease, depression, suicidal tendencies, nytoin, rifAMPin) may decrease
history of drug abuse, respiratory disease, concentration/effects. Strong
biliary tract dysfunction, acute pancreatitis, CYP3A4 inhibitors (e.g., rifAMPin,

Canadian trade name Non-Crushable Drug High Alert drug


752 methadone

clarithromycin, ketoconazole, Dosage in Hepatic Impairment


ritonavir) may increase methadone Mild to moderate impairment: No
level. Amiodarone, voriconazole dose adjustment. Severe Impairment:
may prolong QT interval. MAOIs (e.g., Avoid use.
phenelzine, selegiline) may produce
serotonin syndrome. HERBAL: Herb- Detoxification
als with sedative properties (e.g., PO: ADULTS, ELDERLY: Initially, dose of
chamomile, kava kava, valerian) 20–30 mg. An additional 5–10 mg may be
may increase CNS depression. St. John’s provided if withdrawal symptoms have not
wort may decrease concentration/effect. been suppressed or if symptoms reappear
FOOD: Grapefruit products may alter after 2–4 hrs. Day 1 dose not to exceed 40
concentration/effects. LAB VALUES: May mg. Maintenance range: Titrate to a dose
increase serum amylase, lipase. that prevents withdrawal symptoms for 24
hrs, reduces craving, reduces euphoria effect
AVAILABILITY (Rx) of self-administered opioids, while ensuring
Injection Solution: 10 mg/mL. Oral Con- tolerance to sedative effects of methadone.
centrate: 10 mg/mL. Oral Solution: 5 Usual range: 80–120 mg/day. Dose reduc-
mg/5 mL, 10 mg/5 mL. Tablets, Dispers- tion should be in increments of less than
ible: 40 mg. Tablets: 5 mg, 10 mg. 10% of the maintenance dose every 10–14
days. Short-term: Initially, titrate to 40 mg/
ADMINISTRATION/HANDLING day in 2 divided doses. Continue 40-mg dose
M IM, SQ for 2–3 days. After 2–3 days of stabilization
b ALERT c IM preferred over SQ route at 40 mg, gradually decrease dose to level
(SQ produces pain, local irritation, indu- keeping withdrawal symptoms tolerable.
ration). SIDE EFFECTS
• Do not use if solution appears cloudy
or contains a precipitate. • Administer Frequent: Sedation, orthostatic hypoten-
slowly. • Those with circulatory impair- sion, diaphoresis, facial flushing, con-
ment experience higher risk of overdos- stipation, dizziness, nausea, vomiting.
age due to delayed absorption of re- Occasional: Confusion, urinary retention,
peated administration. palpitations, abdominal cramps, visual
changes, dry mouth, headache, decreased
PO appetite, anxiety, insomnia. Rare: Allergic
• Give without regard to food. • Oral reaction (rash, pruritus).
dose for detoxification and maintenance
may be given in fruit juice or wa- ADVERSE EFFECTS/TOXIC
ter. • Dispersible tablet should not be REACTIONS
chewed or swallowed; add to liquid, al- Overdose results in respiratory depres-
low to dissolve before swallowing. sion, skeletal muscle flaccidity, cold/
clammy skin, cyanosis, extreme drowsi-
INDICATIONS/ROUTES/DOSAGE ness progressing to seizures, stupor,
Analgesia coma. Early sign of toxicity presents
PO: ADULTS, ELDERLY: Initially, 2.5 mg as increased sedation after being on a
q8–12 hrs. May increase by 2.5 mg/ stable dose. Cardiac toxicity manifested
dose or 5 mg/day q5–7 days. as QT prolongation, torsades de pointes.
Tolerance to analgesic effect, physical
Dosage in Renal Impairment dependence may occur with repeated
CrCl less than 10 mL/min: 50–75% nor­ use. Antidote: Naloxone (see Appendix
mal dose. Avoid in severe hepatic disease. J for dosage).

underlined – top prescribed drug


methotrexate 753
an error-prone abbreviation; do
NURSING CONSIDERATIONS not use as an abbreviation.
BASELINE ASSESSMENT
uCLASSIFICATION
Obtain baseline ECG. Assess type, location,
PHARMACOTHERAPEUTIC: Antime-
intensity of pain. Detoxification: Assess pt
for opioid withdrawal. Pt should be in re- tabolite. CLINICAL: Antineoplastic,
cumbent position before drug administra- antirheumatic disease-modifying,
tion by parenteral route. Obtain vital signs immunosuppressant.
before giving medication. If respirations are
12/min or less (20/min or less in children), USES
withhold medication, contact physician.
Oncology-related: Treatment of breast,
INTERVENTION/EVALUATION head/neck, non–small-cell lung, small-cell
Monitor vital signs 15–30 min after SQ/ lung carcinomas; trophoblastic tumors,
IM dose, 5–10 min following IV dose. Oral acute lymphocytic, meningeal leukemias;
medication is 50% as potent as parenteral. non-Hodgkin’s lymphomas (lymphosar-
Assess for adequate voiding. Monitor daily coma, Burkitt’s lymphoma), carcinoma of
pattern of bowel activity, stool consistency. gastrointestinal tract, mycosis fungoides,
Assess for clinical improvement, record osteosarcoma. Non-oncology uses:
onset of relief of pain. Provide support to Psoriasis, rheumatoid arthritis (including
pt in detoxification program; monitor for juvenile idiopathic arthritis). OFF-LABEL:
withdrawal symptoms. Treatment of acute myelocytic leukemia, M
bladder carcinoma, ectopic pregnancy,
PATIENT/FAMILY TEACHING management of abortion, systemic lupus
• Methadone may produce drug de- erythematosus, treatment of and mainte-
pendence, has potential for being nance of remission in Crohn’s disease.
abused. • Avoid alcohol. • Do not
stop taking abruptly after prolonged PRECAUTIONS
use. • May cause dry mouth, drowsi- Contraindications: Hypersensitivity to meth­
ness. • Avoid tasks that require alert- otrexate. Breastfeeding. For pts with pso-
ness, motor skills until response to riasis, juvenile idiopathic arthritis or
drug is established. • Report severe rheumatoid arthritis: Pregnancy, hepatic
drowsiness, respiratory depression. disease, alcoholism, immunodeficiency
syndrome, preexisting blood dyscrasias.
Cautions: Peptic ulcer, ulcerative colitis,
preexisting myelosuppression, history of
methotrexate chronic hepatic disease, alcohol consump-
tion, obesity, diabetes, hyperlipidemia, use
meth-o-trex-ate with other hepatotoxic medications, con-
(Otrexup, Rasuvo, Trexall, Xatmep) comitant use of proton pump inhibitors.
j BLACK BOX ALERT j May Use of NSAIDs or aspirin with lower metho­
cause fetal abnormalities, death. trexate doses for rheumatoid arthritis.
May produce potentially fatal
chronic hepatotoxicity, dermato- ACTION
logic reactions, acute renal failure,
pneumonitis, myelosuppression, Competes with enzymes necessary to
malignant lymphoma, aplastic reduce folic acid to tetrahydrofolic acid,
anemia, GI toxicity. Do not use for a component essential to DNA synthesis,
psoriasis or rheumatoid arthritis
treatment in pregnant women. repair, and cellular replication. Thera-
Do not confuse methotrexate with peutic Effect: Inhibits DNA, protein
metOLazone, methylPREDNISo- synthesis. Possesses anti-inflammatory
lone, or mitoXANTRONE. MTX is and immune-modulating activity.

Canadian trade name Non-Crushable Drug High Alert drug


754 methotrexate

PHARMACOKINETICS ADMINISTRATION/HANDLING
Variably absorbed from GI tract. Com- b ALERT c May be carcinogenic, muta-
pletely absorbed after IM administra- genic, teratogenic. Handle with extreme
tion. Protein binding: 50%–60%. Widely care during preparation/administration.
distributed. Metabolized in liver. Pri- Wear gloves when preparing solution. If
marily excreted in urine. Removed by powder or solution comes in contact
hemodialysis but not by peritoneal dial- with skin, wash immediately, thoroughly
ysis. Half-life: 3–10 hrs (large doses, with soap, water. May give IM, IV, intra-
8–15 hrs). arterially, intrathecally.
LIFESPAN CONSIDERATIONS IV
Pregnancy/Lactation: Avoid pregnancy Reconstitution • Reconstitute powder
during methotrexate therapy and mini- with D5W or 0.9% NaCl to provide con-
mum 3 mos after therapy in males or at centration of 25 mg/mL or less. • For
least one ovulatory cycle after therapy in intrathecal use, dilute with preservative-
females. May cause fetal death, congeni- free 0.9% NaCl to provide a concentration
tal anomalies. Distributed in breast milk. not greater than 2–4 mg/mL.
Breastfeeding not recommended. Chil- Rate of administration • Give IV
dren/Elderly: Renal/hepatic impairment push at rate of 10 mg/min. • Give IV in-
may require dosage ad­just­ment. fusion at rate of 4–20 mg/hr (refer to
specific protocol).
M INTERACTIONS Storage • Store vials at room temper-
DRUG: Alcohol, hepatotoxic medi- ature. Diluted solutions stable for 24 hrs
cations (e.g., acetaminophen, at room temperature.
acitretin) may increase risk of hepa-
totoxicity. Bone marrow depres- IV INCOMPATIBILITIES
sants (e.g., cladribine) may increase Droperidol (Inapsine), gemcitabine (Gem-
myelosuppression. May decrease zar), idarubicin (Idamycin), midazolam
the therapeutic effect of vaccines (Versed), nalbuphine (Nubain).
(live). May increase adverse effects
of natalizumab, vaccines (live). IV COMPATIBILITIES
NSAIDs (e.g., ibuprofen, ketoro- CISplatin (Platinol AQ), cyclophosphamide
lac, naproxen) may increase risk (Cytoxan), DAUNOrubicin (DaunoXome),
of toxicity. Probenecid, salicylates DOXOrubicin (Adriamycin), etoposide
(e.g., aspirin) may increase concen- (VePesid), 5-fluorouracil, granisetron
tration, risk of toxicity. HERBAL: Echi- (Kytril), leucovorin, mitoMYcin (Muta-
nacea may decrease therapeutic effect. mycin), ondansetron (Zofran), PACLitaxel
FOOD: None known. LAB VALUES: May (Taxol), vinBLAStine (Velban), vinCRIStine
increase serum uric acid, AST. (Oncovin), vinorelbine (Navelbine).
AVAILABILITY (Rx) INDICATIONS/ROUTES/DOSAGE
Injection, Powder for Reconstitution: 1 g. Oncology Uses
Injection, Autoinjector: (Rasuvo): 7.5 mg, b ALERT c Refer to individual specific
10 mg, 12.5 mg, 15 mg, 17.5 mg, 20 protocols for optimum dosage, sequence
mg, 22.5 mg, 25 mg, 27.5 mg, 30 mg. of administration.
Injection Solution: 25 mg/mL. Injection,
Syringe: (Otrexup): 7.5 mg/0.4 mL, 10 Head/Neck Cancer
mg/0.4 mL, 15 mg/0.4 mL, 20 mg/0.4 PO, IV, IM: ADULTS, ELDERLY: 40 mg/
mL, 25 mg/0.4 mL. Solution, Oral: (Xat- m2 once wkly. Continue until disease pro-
mep): 2.5 mg/mL. Tablets: 2.5 mg, 5 gression or unacceptable toxicity.
mg, 7.5 mg, 10 mg, 15 mg.
underlined – top prescribed drug
methotrexate 755
Breast Cancer hematemesis. Hepatotoxicity more likely to
IV: ADULTS, ELDERLY:40 mg/m2 days 1 occur with frequent small doses than with
and 8 q4wks in combination with cyclo- large intermittent doses. Pulmonary toxicity
phosphamide and fluorouracil. characterized by interstitial pneumonitis.
Hematologic toxicity, resulting from marked
Mycosis Fungoides myelosuppression, may manifest as leuko-
IM, PO: ADULTS, ELDERLY: 5–50 mg penia, thrombocytopenia, anemia, hemor-
once wkly or 15–37.5 mg twice wkly. rhage. Dermatologic toxicity may produce
Rheumatoid Arthritis (RA)
rash, pruritus, urticaria, pigmentation,
PO: ADULTS: Initially, 10–15 mg once photosensitivity, petechiae, ecchymosis,
wkly. May increase by 5 mg q2–4wks pustules. Severe nephrotoxicity produces
to a maximum dose of 20–30 mg once azotemia, hematuria, renal failure.
weekly. SQ/IM: Initially, 7.5 mg/wk. NURSING CONSIDERATIONS
Adjust dose gradually to optimal response.
ELDERLY: Initially, 5–7.5 mg/wk. Maxi- BASELINE ASSESSMENT
mum: 20 mg/wk. Rheumatoid arthritis: Assess pain, range
of motion. Obtain baseline CBC, BMP, LFT,
Juvenile Rheumatoid Arthritis (JRA) rheumatoid factor. Psoriasis: Assess skin
PO, IM, SQ: CHILDREN: Initially, 10
mg/ lesions. Question for possibility of preg-
m2 once wkly, then 20–30 mg/m2/wk as nancy in pts with psoriasis, rheumatoid
a single dose. arthritis (RA). Obtain all functional tests M
Psoriasis
before therapy, repeat throughout therapy.
PO: ADULTS, ELDERLY: Initially, 10–25 mg Antiemetics may prevent nausea, vomiting.
once wkly or 2.5–5 mg q12h for 3 doses INTERVENTION/EVALUATION
once wkly. IM/SQ: 10–25 mg once wkly. Monitor CBC, BMP, LFT, urinalysis, chest X-
Adjust dose gradually to optimal response. rays, serum uric acid. Monitor for hema-
Titrate to lowest effective dose. tologic toxicity (fever, sore throat, signs of
Dosage in Renal Impairment
local infection, unusual bruising/bleeding
from any site), symptoms of anemia (ex-
Creatinine Clearance Reduce Dose to
cessive fatigue, weakness). Assess skin for
61–80 mL/min 75% of normal evidence of dermatologic toxicity. Keep pt
51–60 mL/min 70% of normal
10–50 mL/min 30–50% of normal
well hydrated, urine alkaline. Avoid rectal
Less than 10 mL/min Avoid use temperatures, traumas that induce bleed-
ing. Apply 5 full min of pressure to IV sites.
Dosage in Hepatic Impairment
PATIENT/FAMILY TEACHING
Use caution.
• Maintain strict oral hygiene. • Do not
SIDE EFFECTS have immunizations without physician’s ap-
Frequent (10%–3%): Nausea, vomiting, sto- proval (drug lowers resistance). • Avoid
matitis, burning/erythema at psoriatic site crowds, those with infection. • Avoid al-
(in pts with psoriasis). Occasional (3%– cohol, aspirin. • Avoid ultraviolet sunlight
1%): Diarrhea, rash, dermatitis, pruritus, exposure. • Use contraceptive measures
alopecia, dizziness, anorexia, malaise, during therapy and for 3 mos (males) or 1
headache, drowsiness, blurred vision. ovulatory cycle (females) after ther-
apy. • Promptly report fever, sore throat,
ADVERSE EFFECTS/TOXIC signs of local infection, unusual bruising/
REACTIONS bleeding from any site, diarrhea. • Hair
High potential for various severe tox- loss is reversible, but new hair growth may
icities. GI toxicity may produce gingivitis, have different color, texture. • Report
glossitis, pharyngitis, stomatitis, enteritis, persistent nausea/vomiting.
Canadian trade name Non-Crushable Drug High Alert drug
756 methylergonovine
distributed in breast milk. Children/
methylergonovine Elderly: No information available.

meth-il-er-goe-noe-veen INTERACTIONS
(Methergine ) DRUG: May increase hypertensive effect
of DOPamine, ­norepinephrine,
uCLASSIFICATION
phenylephrine, vasopressin. Strong
PHARMACOTHERAPEUTIC: Ergot CYP3A4 inhibitors (e.g., clarithro-
alkaloid. CLINICAL: Oxytocic agent, mycin, ketoconazole, ritonavir)
uterine stimulant. may increase concentration/effect. Beta
blockers (e.g., carvedilol, labet-
alol, metoprolol) may increase vaso-
USES
constrictive effect of ergot derivatives.
Management of uterine atony, hemor- May decrease vasodilation effect of
rhage and subinvolution of uterus follow- nitroglycerin. May increase vasocon-
ing delivery of placenta. Control uterine stricting effect of serotonin 5-HT1D
hemorrhage following delivery of ante- receptor agonists (e.g., SUMAt-
rior shoulder in second stage of labor. riptan). HERBAL: None significant.
FOOD: None known. LAB VALUES: May
PRECAUTIONS
decrease serum prolactin.
Contraindications: Hypersensitivity to meth-
M ylergonovine. Hypertension, pregnancy, tox- AVAILABILITY (Rx)
emia. Cautions: Renal/hepatic impairment, Injection Solution: 0.2 mg/mL. Tablets:
coronary artery disease, pts at risk for coro- 0.2 mg.
nary artery disease (diabetes, obesity, smok-
ing, hypercholesterolemia), concurrent use ADMINISTRATION/HANDLING
with CYP3A4 inhibitors (e.g., protease inhi­ Reconstitution • Dilute with 0.9%
bitors), occlusive peripheral vascular dis- NaCl to volume of 5 mL.
ease, sepsis, second stage of labor. Rate of administration • Give over
at least 1 min, carefully monitoring B/P.
ACTION
Storage • Refrigerate ampules.
Increases tone, rate, amplitude of con-
traction of uterine smooth muscle. IV INCOMPATIBILITIES
Therapeutic Effect: Produces sustained None known.
contractions, which shortens third stage
of labor, reduces blood loss. IV COMPATIBILITIES
Heparin, potassium.
PHARMACOKINETICS
Route Onset Peak Duration INDICATIONS/ROUTES/DOSAGE
PO 5–10 min N/A 3 hrs Prevention/Treatment of Postpartum,
IV Immediate N/A 45 min Postabortion Hemorrhage
IM 2–5 min N/A 3 hrs PO: ADULTS: 0.2 mg 3–4 times daily.
Rapidly absorbed from GI tract after Continue for up to 7 days.
IM administration. Distributed rapidly IV, IM: ADULTS: Initially, 0.2 mg after
to plasma, extracellular fluid, tissues. delivery of anterior shoulder, after delivery
Metabolized in liver. Primarily excreted of placenta, or during puerperium. May
in urine. Half-life: 0.5–2 hrs. repeat q2–4h as needed.
Note: Initial dose may be given parenter-
LIFESPAN CONSIDERATIONS ally, followed by oral regimen.
Pregnancy/Lactation: Contraindi- IV use in life-threatening emergencies
cated during pregnancy. Small amounts only.

underlined – top prescribed drug


methylnaltrexone 757
Dosage in Renal/Hepatic Impairment USES
Use caution. Injection: Treatment of opioid-induced
SIDE EFFECTS constipation in pts with advanced illness
or pain caused by active cancer who
Frequent: Nausea, uterine cramping, require opioid dosage escalation for pal-
vomiting. Occasional: Abdominal pain, liative care. Injection/Tablets: Treat-
diarrhea, dizziness, diaphoresis, tinnitus, ment of opioid-induced constipation in
bradycardia, chest pain. Rare: Aller- pts with chronic pain unrelated to cancer.
gic reaction (rash, pruritus), dyspnea,
severe or sudden hypertension. PRECAUTIONS
ADVERSE EFFECTS/TOXIC Contraindications: Hypersensitivity to meth­
REACTIONS y­lnaltrexone. Known or suspected GI obstr­
uction. Pts at increased risk of recurrent
Severe hypertensive episodes may result in GI obstruction. Cautions: Renal impair-
CVA, serious arrhythmias, seizures. Hyperten- ment, history of GI tract lesions (e.g., peptic
sive effects are more frequent with pt suscep- ulcer disease, GI tract malignancies).
tibility, rapid IV administration, concurrent
use of regional anesthesia, vasoconstrictors. ACTION
Peripheral ischemia may lead to gangrene. Blocks binding of opioids to peripheral opi-
NURSING CONSIDERATIONS oid receptors within GI tract. Inhibits opioid-
induced decreased GI motility and delay
BASELINE ASSESSMENT in GI transit time. Therapeutic Effect: M
Determine baseline serum calcium level, Decre­ases constipating effect of opioids.
B/P, pulse. Assess for any evidence of
bleeding before administration. PHARMACOKINETICS
Absorbed rapidly. Undergoes moder-
INTERVENTION/EVALUATION ate tissue distribution. Protein binding:
Monitor uterine tone, bleeding, B/P, pulse 11%–15%. Excreted in urine (50%),
q15min until stable (about 1–2 hrs). Assess feces (35%). Half-life: 8 hrs.
extremities for color, warmth, movement,
pain. Report chest pain promptly. Provide LIFESPAN CONSIDERATIONS
support with ambulation if dizziness occurs. Pregnancy/Lactation: Unknown if
distributed in breast milk (not recom-
PATIENT/FAMILY TEACHING
mended). Children: Safety and efficacy
• Avoid smoking: causes increased not established. Elderly: No age-related
vasoconstriction. • Report increased precautions noted.
cramping, bleeding, foul-smelling lo-
chia. • Report pale, cold hands/feet INTERACTIONS
(possibility of diminished circulation). DRUG: May increase adverse/toxic effects
of naloxegol, opioid antagonists.
HERBAL: None significant. FOOD: None
methylnaltrexone known. LAB VALUES: None significant.

meth-il-nal-trex-own AVAILABILITY (Rx)


(Relistor) Injection Solution: 8 mg/0.4 mL, 12 mg/0.6
Do not confuse methylnaltrexone mL. Tablets: 150 mg.
with naltrexone.
ADMINISTRATION/HANDLING
uCLASSIFICATION PO
PHARMACOTHERAPEUTIC: Opioid rece­ • Administer with water on an empty stom-
ptor antagonist. CLINICAL: GI agent. ach at least 30 min before first meal of day.

Canadian trade name Non-Crushable Drug High Alert drug


758 methylphenidate
SQ
Preparation • Visually inspect for par- NURSING CONSIDERATIONS
ticulate matter or discoloration. Solution BASELINE ASSESSMENT
should appear colorless to pale yellow in
Question characteristics of constipation, fre-
color. Do not use if solution is cloudy, dis-
quency of bowel movements. Assess bowel
colored, or if large particles are observed.
sounds. Question history of GI obstruction,
Administration • Insert needle sub-
perforation, baseline GI disease; renal im-
cutaneously into upper arms, outer thigh,
pairment. Receive full medication history,
or abdomen, and inject solution. • Do
including herbal products, and screen
not inject into areas of active skin disease
for interactions. Assess hydration status.
or injury such as sunburns, skin rashes,
inflammation, skin infections, or active INTERVENTION/EVALUATION
psoriasis. • Rotate injection sites. 30% of pts report defecation within 30 min
Storage • Once solution is drawn into after drug administration. Encourage fluid
syringe, may be stored at room tempera- intake. Assess bowel sounds for peristal-
ture. • Administer within 24 hrs. sis. Monitor daily pattern of bowel activity,
stool consistency. If opioid medication is
INDICATIONS/ROUTES/DOSAGE
stopped, drug should be discontinued. As-
b ALERT c Usual schedule is once ev- sess for abdominal disturbances.
ery other day, as needed, but no more
frequently than once every 24 hrs. PATIENT/FAMILY TEACHING
M • Laxative effect usually occurs within
Constipation (Chronic Non-Cancer Pain) 30 min but may take up to 24 hrs after
PO: ADULTS, ELDERLY: 450 mg once medication administration. • Common
daily in the morning. SQ: ADULTS, side effects include transient abdominal
ELDERLY: 12 mg/day. Note: Discontinue pain, nausea, vomiting. • Report per-
all laxatives prior to use. sistent or worsening symptoms, or if se-
vere or persistent diarrhea occurs.
Constipation (Advanced Illness)
SQ: ADULTS, ELDERLY WEIGHING 38 KG TO
LESS THAN 62 KG: 8 mg. ADULTS, ELDERLY
WEIGHING 62–114 KG: 12 mg. ADULTS, methylphenidate
ELDERLY WHOSE WEIGHT FALLS OUTSIDE
THESE RANGES: Dose at 0.15 mg/kg (round meth-il-fen-i-date
dose up to nearest 0.1 mL of volume). (Aptensio XR, Concerta, Cotempla
XR, Daytrana, Metadate ER, Methylin,
Dosage in Severe Renal Impairment (CrCl Quillichew ER, Quillivant XR, Ritalin,
Less Than 60 mL/min) Ritalin LA)
SQ: ADULTS, ELDERLY: Administer 50% j BLACK BOX ALERT jChronic
of recommended dose. abuse can lead to marked tolerance,
psychological dependence. Abrupt
Dosage in Hepatic Impairment withdrawal from prolonged use may
No dose adjustment. lead to severe depression, psychosis.
Do not confuse Metadate ER
SIDE EFFECTS with Metadate CD, methylpheni-
Frequent (29%–12%): Abdominal pain, flat- date with methadone, or Ritalin
ulence, nausea. Occasional (7%–5%): Diar- with Rifadin.
rhea, dizziness. uCLASSIFICATION
ADVERSE EFFECTS/TOXIC PHARMACOTHERAPEUTIC: CNS
REACTIONS stimulant (Schedule II). CLINICAL:
None known. CNS stimulant.

underlined – top prescribed drug


methylphenidate 759

USES children younger than 6 yrs. Elderly: No


Treatment of attention-deficit hyperactivity age-related precautions noted.
disorder (ADHD). Management of narco-
INTERACTIONS
lepsy. OFF-LABEL: Secondary mental depres-
sion (especially elderly pts, medically ill). DRUG: MAOIs (e.g., phenelzine, sele-
giline) may increase hypertensive effects.
PRECAUTIONS Other CNS stimulants (e.g., caffeine,
Contraindications: Hypersensitivity to meth- dextroamphetamine, phentermine)
ylphenidate. Use during or within 14 days may have additive effect. May inhibit metab-
following MAOI therapy; marked anxiety, olism of warfarin, anticonvulsants
tension, agitation, motor tics; family history (e.g., carBAMazepine, phenytoin),
or diagnosis of Tourette’s syndrome, glau- antidepressants. Alcohol may increase
coma. Metadate: Severe hypertension, HF, adverse effects. HERBAL: Ephedra may
arrhythmia, hyperthyroidism, recent MI or cause hypertension, arrhythmias. Yohimbe
angina. Cautions: Hypertension, seizures, may increase CNS stimulation. FOOD: None
acute stress reaction, emotional instability, known. LAB VALUES: None significant.
history of drug dependence, HF, recent MI,
AVAILABILITY (Rx)
hyperthyroidism or thyrotoxicosis, known
structural cardiac abnormality, bipolar Oral Solution: (Methylin): 5 mg/5 mL, 10
disorder, cardiomyopathy, arrhythmias, mg/5 mL, 10 mg/1 mL. Tablets, Chewable:
alcohol abuse. (Methylin): 2.5 mg, 5 mg, 10 mg. Tablets:
(Methylin, Ritalin): 5 mg, 10 mg, 20 mg. M
ACTION Topical Patch: (Daytrana): 10 mg/9 hrs,
Blocks reuptake of norepinephrine, dopa- 15 mg/9 hrs, 20 mg/9 hrs, 30 mg/9 hrs.
mine into presynaptic neurons. Stimulates Powder for Suspension, Extended-Release:
cerebral cortex and subcortical structures. (Quillivant XR): 25 mg/5 mL. Capsules,
Therapeutic Effect: Decreases motor Extended-Release 24 hr: (Aptensio XR): 10
restlessness, fatigue. Increases motor activ- mg, 15 mg, 20 mg, 30 mg, 40 mg, 50 mg, 60
ity, attention span, mental alertness. Pro- mg. Capsules, Extended-Release: 10 mg, 20
duces mild euphoria. mg, 30 mg, 40 mg, 50 mg, 60 mg. Capsules,
Extended-Release 24 hr: (Ritalin LA): 10 mg,
PHARMACOKINETICS 20 mg, 30 mg, 40 mg. Tablets, Extended-
Onset Peak Duration Release: (Concerta): 18 mg, 27 mg, 36 mg,
Immediate-release 2 hrs 3–6 hrs
54 mg, 72 mg. Tablets: Extended-Release:
Sustained-release 4–7 hrs 8 hrs (Metadate ER, Methylin ER): 10 mg, 20
Extended-release N/A 12 hrs mg. Tablets, Extended-Release: (Quillichew
Transdermal 2 hrs N/A ER): 20 mg, 30 mg, 40 mg.
Capsules, Extended-Release: (Ap-
Slowly, incompletely absorbed from GI tensio XR): 10 mg, 15 mg, 20 mg, 30
tract. Protein binding: 15%. Metabo- mg, 40 mg, 50 mg, 60 mg. Capsules,
lized in liver. Primarily excreted in urine. Extended-Release: 10 mg, 20 mg, 30 mg,
Unknown if removed by hemodialysis. 40 mg, 50 mg, 60 mg. Extended-­Release:
Half-life: 2–4 hrs. (Ritalin LA): 10 mg, 20 mg, 30 mg, 40
LIFESPAN CONSIDERATIONS mg. Tablets, Extended-Release: (Con-
certa): 18 mg, 27 mg, 36 mg, 54 mg, 72
Pregnancy/Lactation: Unknown if mg. (Metadate ER, Methylin ER): 10 mg,
drug crosses placenta or is distributed in 20 mg. Sustained-Release: (Ritalin SR): 20
breast milk. Children: May be more sus- mg. Tablets, Extended-Release ODT: (Co-
ceptible to developing anorexia, insomnia, templa XR): 8.6 mg, 17.3 mg, 25.9 mg.
stomach pain, decreased weight. Chronic Tablets, Chewable, Extended-Release:
use may inhibit growth. Not approved for (Quillichew ER): 20 mg, 30 mg, 40 mg.

Canadian trade name Non-Crushable Drug High Alert drug


760 methylphenidate

ADMINISTRATION/HANDLING AGE: Initially, 18 mg once daily; may


b ALERT c Sustained-release, extended- increase by 18 mg/day at wkly intervals.
release tablets may be given in place of Maximum: 54 mg/day in children 6–12
regular tablets once the daily dose is ti- yrs of age (up to 72 mg/day in adoles-
trated using regular tablets and the titrated cents younger than 18 yrs).
dosage corresponds to sustained-release PO: (Metadate CD): CHILDREN 6 YRS AND
or extended-release tablet strength. OLDER: Initially, 20 mg/day. May increase
by 10–20 mg/day at wkly intervals. Maxi-
PO mum: 60 mg/day.
• Do not give in afternoon or evening (may PO: (Quillichew ER): CHILDREN 6 YRS
cause insomnia). • Do not crush, break AND OLDER: Initially, 20 mg/day. May
extended-release capsules, extended- or increase by 10 mg, 15 mg or 20 mg/day
sustained-release tablets. • Immediate- at wkly intervals. Maximum: 60 mg/day.
release tablets may be crushed. • Give PO: (Quillivant XR): CHILDREN 6 YRS AND
dose 30–45 min before meals. • Con- OLDER: Initially, 20 mg once daily in the
certa: Administer once daily in morning. morning. May increase in increments of
May take without regard to food but must 10–20 mg/day at wkly increments. Maxi-
be taken with water, milk, or juice. • Me- mum: 60 mg/day.
thylin Chewable: Give with at least 8 oz PO: (Ritalin LA): CHILDREN 6 YRS AND
of water or other fluid. • Metadate CD, OLDER:Initially, 20 mg/day. May increase
Ritalin LA: • May be ope­ned, sprinkled by 10 mg/day at wkly intervals. Maxi-
M on applesauce. • Instruct pt to swallow mum: 60 mg/day.
applesauce without chewing. Do not crush PO: (Metadate ER, Methylin ER):
or chew capsule contents. • Quillivant CHILDREN 6 YRS AND OLDER: May replace
XR: Administer in morning with or with- regular tablets after daily dose is titrated
out food. Shake bottle more than 10 sec and 8-hr dosage corresponds to sus-
prior to administration. tained-release or extended-release tablet
strength. Maximum: 60 mg/day.
Patch PO: (Cotempla XR): CHILDREN, 6–18
• To be worn daily for 9 hrs. • Re- YRS: Initially, 17.3 mg once daily. May
place daily in morning. • Apply to dry, increase in wkly intervals in 8.6 to 17.3
clean area of hip. • Avoid applying to mg increments. Maximum: 51.8 mg/
waistline (clothing may cause patch to day.
rub off). • Alternate application site Patch: (Daytrana): CHILDREN 6–12 YRS,
daily. • Press firmly in place for 30 sec ADOLESCENTS: Initially, 10 mg daily
to ensure patch is in good contact with (applied and worn for 9 hrs). Dos-
skin. • Do not cut patch. age is titrated to desired effect. May
increase dose no more frequently than
INDICATIONS/ROUTES/DOSAGE every wk.
ADHD
PO: ADULTS: (Immediate-Release): 5 Narcolepsy
mg twice daily, before breakfast and lunch. PO: ADULTS, ELDERLY: (Immediate-
May increase by 5–10 mg/day at wkly inter- Release): Initially, 5 mg twice daily,
vals. Maximum: 60 mg/day in 2–3 divided before breakfast and lunch. May increase
doses. CHILDREN 6 YRS AND OLDER: Initially, by 5–10 mg/day at wkly intervals. Maxi-
2.5–5 mg before breakfast and lunch. May mum: 60 mg/day in 2–3 divided doses.
increase by 5–10 mg/day at wkly inter- (Extended-Release): May be given once
vals. Usual dose: 20–30 mg/day in 2–3 the immediate-release dose is titrated and
divided doses. Maximum: 60 mg/day. the titrated 8-hr dose corresponds to sus-
PO: (Concerta): CHILDREN 6 YRS tained-release or extended-release tablet
AND OLDER, ADULTS UP TO 65 YRS OF strength. Maximum: 60 mg/day.

underlined – top prescribed drug


methylPREDNISolone 761
Dosage in Renal/Hepatic Impairment
No dose adjustment. methylPREDNISolone
SIDE EFFECTS meth-il-pred-nis-oh-lone
Frequent: Anxiety, insomnia, anorexia. (Medrol)
Occasional: Dizziness, drowsiness, head-
ache, nausea, abdominal pain, fever, rash, methylPREDNISolone
arthralgia, vomiting. Rare: Blurred vision,
Tourette’s syndrome (uncontrolled vocal acetate
outbursts, repetitive body movements,
tics), palpitations, priapism. (DepoMedrol)

ADVERSE EFFECTS/TOXIC
REACTIONS
methylPREDNISolone
Prolonged administration to children sodium succinate
with ADHD may delay normal weight gain
pattern. Overdose may produce tachy- (SOLU-MEDROL)
cardia, palpitations, arrhythmias, chest Do not confuse DepoMedrol
pain, psychotic episode, seizures, coma. with Solu-Medrol, Medrol with
Hypersensitivity reactions, blood dyscra- Mebaral, or methylPREDNISo-
sias occur rarely. lone with medroxyPROGESTER-
one or prednisoLONE. M
NURSING CONSIDERATIONS
uCLASSIFICATION
BASELINE ASSESSMENT
PHARMACOTHERAPEUTIC: Adrenal
ADHD: Assess attention span, impul- corti­costeroid. CLINICAL: Anti-inflam­
sivity, interaction with others, distract- matory.
ibility. Narcolepsy: Observe/assess
frequency of episodes. Question history
of seizures. USES
Anti-inflammatory or immunosuppres-
INTERVENTION/EVALUATION
sant in the treatment of hematologic,
Monitor B/P, pulse, changes in ADHD allergic, neoplastic, dermatologic, endo-
symptoms. CBC with differential should crine, GI, nervous system, ophthalmic,
be performed routinely during therapy. renal, or rheumatic disorders. OFF-
If paradoxical return of attention-deficit LABEL: Acute spinal cord injury.
occurs, dosage should be reduced or dis-
continued. Monitor growth. PRECAUTIONS
PATIENT/FAMILY TEACHING
Contraindications: Hypersensitivity
to methylprednisolone. Administration
• Avoid tasks that require alertness, mo- of live or attenuated virus vaccines, sys-
tor skills until response to drug is estab- temic fungal infection. IM: Idiopathic
lished. • Sugarless gum, sips of water thrombocytopenia purpura. Intrathecal
may relieve dry mouth. • Report any administration. Cautions: Respiratory
increase in seizures. • Take daily dose tuberculosis, untreated systemic infections,
early in morning to avoid insom- hypertension, HF, diabetes, GI disease (e.g.,
nia. • Report anxiety, palpitations, fe- peptic ulcer), myasthenia gravis, renal/
ver, vomiting, skin rash. • Report new hepatic impairment, seizures, cataracts,
or worsened symptoms (e.g., behavior, glaucoma, following acute MI, thyroid
hostility, concentration ability). • Avoid disorder, thromboembolic tendencies, car-
caffeine. • Do not stop taking abruptly diovascular disease, elderly pts, psychiatric
after prolonged use. conditions, pts at risk for osteoporosis.
Canadian trade name Non-Crushable Drug High Alert drug
762 methylPREDNISolone

ACTION AVAILABILITY (Rx)


Anti-inflammatory: Suppresses migra- Injection, Powder for Reconstitution:
tion of polymorphonuclear leukocytes, (SOLU): 40 mg, 125 mg, 500 mg, 1 g.
reverses increased capillary permeability. Injection, Suspension: (DEPO): 20 mg/mL,
Exerts effects on modulating carbohy- 40 mg/mL, 80 mg/mL. Tablets: (Medrol): 2
drate, protein, lipid metabolism. Maintains mg, 4 mg, 8 mg, 16 mg, 32 mg. (Medrol
fluid/electrolyte hemostasis. Influences CV, Dosepak): 4 mg (21 tablets).
immunologic, endocrine, musculoskel-
etal, neurologic physiology. Therapeutic ADMINISTRATION/HANDLING
Effect: Decreases inflammation. b ALERT c Do not give methylPRED-
NIsolone acetate IV.
PHARMACOKINETICS
IV
Route Onset Peak Duration
PO Rapid 1–2 hrs 30–36 hrs Reconstitution • For infusion, add to
IM Rapid 4–8 days 1–4 wks D5W, 0.9% NaCl.
IV Rapid N/A N/A Rate of administration • Give IV
push over 3–15 min. • Give IV piggy-
Well absorbed from GI tract after IM back. Dose of 250 mg over 15–30 min;
administration. Widely distributed. Metab- dose of 500–999 mg over at least 30 min;
olized in liver. Excreted in urine. Removed dose of 1g or greater over 1 hr.
by hemodialysis. Half-life: 3.5 hrs. Storage • Store vials at room temper-
M ature. Diluted solution is stable for 48
LIFESPAN CONSIDERATIONS hrs at room temperature or refrigerated.
Pregnancy/Lactation: Crosses placenta.
Distributed in breast milk. May cause cleft pal- IM
ate (chronic use in first trimester). Breastfeed- • MethylPREDNISolone acetate should not
ing not recommended. Children: Prolonged be further diluted. • MethylPREDNISo-
treatment or high dosages may decrease lone sodium succinate should be reconsti-
short-term growth rate, cortisol secretion. tuted with Bacteriostatic Water for Injec-
Elderly: No age-related precautions noted. tion. • Give deep IM in gluteus maximus
(avoid injection into deltoid muscle).
INTERACTIONS
DRUG: May increase anticoagulant effects of PO
warfarin. Strong CYP3A inducers (e.g., • Give with food, milk.
carBAMazepine, phenytoin, rifAMPin)
may decrease effects. Live virus vaccines IV INCOMPATIBILITIES
may decrease pt’s antibody response to vac- Ciprofloxacin (Cipro), dilTIAZem (Cardi-
cine, increase vaccine side effects, potentiate zem), potassium chloride, propofol
virus replication. May increase hyponatremic (Diprivan).
effect of desmopressin. Strong CYP3A4
inhibitors (e.g., clarithromycin, keto- IV COMPATIBILITIES
conazole, ritonavir) may increase con- Dexmedetomidine (Precedex), DOPa-
centration/effect. HERBAL: Herbals with mine (Intropin), heparin, midazolam
sedative properties (e.g., chamomile, (Versed), theophylline.
kava kava, valerian) may increase CNS
depression. St. John’s wort may decrease INDICATIONS/ROUTES/DOSAGE
concentration. FOOD: None known. LAB VAL- Anti-inflammatory, Immunosuppressive
UES: May increase serum glucose, choles- IV: ADULTS, ELDERLY: 10–40 mg. May repeat
terol, lipids, amylase, sodium. May decrease q4–6h as needed. CHILDREN: Initially, 0.11–
serum calcium, potassium, thyroxine, hypo- 1.6 mg/kg/day in 3–4 divided doses. Range:
thalamic-pituitary-adrenal (HPA) axis. 0.5–1.7 mg/kg/day in 2–4 divided doses.

underlined – top prescribed drug


metoclopramide 763
PO: ADULTS, ELDERLY: 4–48 mg/day in at least twice daily. Be alert for infection
1–4 divided doses. CHILDREN: 0.5–1.7 (sore throat, fever, vague symptoms).
mg/kg/day or 5–25 mg/m2/day in 2–4 Monitor serum electrolytes, including
divided doses. B/P, glucose. Monitor for hypocalcemia
IM: (MethylPREDNISolone Succinate): (muscle twitching, cramps, positive
ADULTS, ELDERLY: 10–40 mg/day. Trousseau’s or Chvostek’s signs), hy-
IM: (Methylprednisolone Acetate): pokalemia (weakness, muscle cramps,
ADULTS, ELDERLY: 4–120 mg single dose. numbness, tingling [esp. lower extremi-
Intra-articular, intralesional: ADULTS, ties], nausea/vomiting, irritability, ECG
ELDERLY: 4–80 mg q1–5wks. changes). Assess emotional status, ability
to sleep. Check lab results for blood co-
Dosage in Renal/Hepatic Impairment agulability, clinical evidence of thrombo-
No dose adjustment. embolism.
SIDE EFFECTS PATIENT/FAMILY TEACHING
Frequent: Insomnia, heartburn, anxiety, • Take oral dose with food, milk. • Do
abdominal distention, diaphoresis, acne, not change dose/schedule or stop taking
mood swings, increased appetite, facial drug; must taper off gradually under medi-
flushing, GI distress, delayed wound cal supervision. • Report fever, sore
healing, increased susceptibility to throat, muscle aches, sudden weight gain
infection, diarrhea, constipation. Occa- or loss, edema, loss of appetite, fatigue.
sional: Headache, edema, tachycardia, • Maintain strict personal hygiene; avoid M
change in skin color, frequent urination, exposure to disease, trauma. • Severe
depression. Rare: Psychosis, increased stress (serious infection, surgery, trauma)
blood coagulability, hallucinations. may require increased dosage. • Follow-
up visits, lab tests are necessary.
ADVERSE EFFECTS/TOXIC • Children must be assessed for growth
REACTIONS retardation. • Inform dentist, other physi-
Long-term therapy: Hypocalcemia, cians of methylprednisolone therapy now
hypokalemia, muscle wasting (esp. in arms, or within past 12 mos.
legs), osteoporosis, spontaneous fractures,
amenorrhea, cataracts, glaucoma, pep-
tic ulcer, HF. Abrupt withdrawal after
long-term therapy: Anorexia, nausea, metoclopramide
fever, headache, severe arthralgia, rebound
inflammation, fatigue, weakness, lethargy, met-oh-kloe-pra-myde
dizziness, orthostatic hypotension. (Metonia , Reglan)
j BLACK BOX ALERT jProlonged
NURSING CONSIDERATIONS use may cause tardive dyskinesia.
Do not confuse metoclopramide
BASELINE ASSESSMENT with metOLazone or metopro-
Question for hypersensitivity to any of the lol, or Reglan with Renagel.
corticosteroids, components. Obtain base-
lines for height, weight, B/P, serum glucose, uCLASSIFICATION
electrolytes. Check results of initial tests PHARMACOTHERAPEUTIC: DOPa-
(tuberculosis [TB] skin test, X-rays, ECG). mine, serotonin receptor antagonist.
Question history as listed in Precautions. CLINICAL: GI agent, antiemetic.

INTERVENTION/EVALUATION
Monitor I&O, daily weight; assess for USES
edema. Monitor daily pattern of bowel ac- PO: Symptomatic treatment of diabe­tic
tivity, stool consistency. Check vital signs gastroparesis, gastroesophageal reflux.
Canadian trade name Non-Crushable Drug High Alert drug
764 metoclopramide
IV/IM: Symptomatic treatment of diabetic tricyclic antidepressants (e.g., ami-
gastroparesis, prevent/treat nausea/vomit- triptyline, doxepin). Strong CYP2D6
ing with chemotherapy or after surgery. inhibitors (e.g., FLUoxetine, PAR-
oxetine) may increase concentra-
PRECAUTIONS tion/effect. HERBAL: None significant.
Contraindications: Hypersensitivity to meto- FOOD: None known. LAB VALUES: May
clopramide. Concurrent use of medications increase serum aldosterone, prolactin.
likely to produce extrapyramidal reac-
tions. Situations in which GI motility may be AVAILABILITY (Rx)
dangerous (e.g., GI hemorrhage, GI perfo- Injection Solution: 5 mg/mL. Solution,
ration/obstruction), history of seizure disor- Oral: 5 mg/5 mL. Tablets: 5 mg, 10 mg.
der, pheochromocytoma. Cautions: Renal Tablets, Orally Disintegrating: 5 mg,
impairment, HF, cirrhosis, hypertension, 10 mg.
depression, Parkinson’s disease, elderly.
ADMINISTRATION/HANDLING
ACTION
IV
Blocks dopamine/serotonin receptors in
chemoreceptor trigger zone of the CNS. Reconstitution • Dilute doses greater
Enhances acetylcholine response in upper than 10 mg in 50 mL D5W or 0.9% NaCl.
GI tract, causing increased motility and Rate of administration • Infuse over
accelerated gastric emptying without stimu- 15–30 min. • May give undiluted slow
M lating gastric, biliary, or pancreatic secre- IV push at rate of 10 mg over 1–2
tions; increases lower esophageal sphincter min. • Too-rapid IV injection may pro-
tone. Therapeutic Effect: Accelerates duce intense feeling of anxiety, restless-
intestinal transit, promotes gastric empty- ness, followed by drowsiness.
ing. Relieves nausea, vomiting. Storage • Store vials at room temper-
ature. • After dilution, IV infusion (pig-
PHARMACOKINETICS gyback) is stable for 24 hrs.
Route Onset Peak Duration
PO 30–60 min N/A 1–2 hrs PO
IV 1–3 min N/A 1–2 hrs • Give 30 min before meals and at bed-
IM 10–15 min N/A 1–2 hrs time. • Tablets may be crushed. • Do
not cut, divide, break orally disintegrating
Well absorbed from GI tract. Metabolized tablets. Place on tongue, swallow with saliva.
in liver. Protein binding: 30%. Primarily
excreted in urine. Not removed by hemo- IV INCOMPATIBILITIES
dialysis. Half-life: 4–6 hrs. Allopurinol (Aloprim), cefepime (Maxi­pime),
furosemide (Lasix), propofol (Diprivan).
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses placenta. IV COMPATIBILITIES
Distributed in breast milk. Children: More Dexamethasone, dexmedetomidine (Pre-
susceptible to having dystonic reactions. cedex), dilTIAZem (Cardizem), diphenhy-
Elderly: More likely to have parkinsonian drAMINE (Benadryl), fentaNYL (Sublimaze),
dyskinesias after long-term therapy. heparin, HYDROmorphone (Dilaudid),
morphine, potassium chloride.
INTERACTIONS
DRUG: May increase adverse effects of INDICATIONS/ROUTES/DOSAGE
antipsychotic (e.g., haloperidol), Prevention of Chemotherapy-Induced
promethazine, SNRIs (e.g., DULox- Nausea/Vomiting
etine, venlafaxine), SSRIs (e.g., PO: ADULTS, ELDERLY: 10 mg q6h prn.
citalopram, PARoxetine), tramadol,

underlined – top prescribed drug


metOLazone 765
Diabetic Gastroparesis INTERVENTION/EVALUATION
PO, IV: ADULTS, ELDERLY: 5–10 mg 30 Monitor for anxiety, restlessness, extra-
min before meals and at bedtime for up pyramidal symptoms (EPS) during IV
to 12 wks. administration. Monitor daily pattern of
bowel activity, stool consistency. Assess
Dosage in Renal Impairment
skin for rash. Evaluate for therapeutic re-
Dosage is modified based on creatinine sponse from gastroparesis (nausea, vomit-
clearance. ing, bloating). Monitor renal function, B/P,
Creatinine Clearance Dosage heart rate.
Less than 40 mL/min 50% of normal dose
PATIENT/FAMILY TEACHING
Dosage in Hepatic Impairment • Avoid tasks that require alertness, mo-
No dose adjustment. tor skills until response to drug is estab-
lished. • Report involuntary eye, facial,
SIDE EFFECTS limb movement (extrapyramidal reac-
b ALERT c Doses of 2 mg/kg or greater, tion). • Avoid alcohol.
or increased length of therapy, may result
in a greater incidence of side effects.
Frequent (10%): Drowsiness, restlessness,
fatigue, lethargy. Occasional (3%): Dizzi- metOLazone
ness, anxiety, headache, insomnia, breast
tenderness, altered menstruation, con- meh-toe-la-zone M
stipation, rash, dry mouth, galactorrhea, (Zaroxolyn )
gynecomastia. Rare (less than 3%): Hypo- Do not confuse metOLazone
tension, hypertension, tachycardia. with metaxalone, m
­ ethotrexate,
metoclopramide, or meto-
ADVERSE EFFECTS/TOXIC prolol, or Zaroxolyn with
REACTIONS Zarontin.
Extrapyramidal reactions occur most
frequently in children, young adults uCLASSIFICATION
(18–30 yrs) receiving large doses (2 PHARMACOTHERAPEUTIC: Thiazide
mg/kg) during chemotherapy and usu- diuretic. CLINICAL: Diuretic, antihy-
ally are limited to akathisia (involuntary pertensive.
limb movement, facial grimacing, motor
restlessness). Neuroleptic malignant
syndrome (diaphoresis, fever, unsta- USES
ble B/P, muscular rigidity) has been Treatment of mild to moderate hyperten-
reported. sion, edema due to HF, nephrotic syn-
drome, or impaired renal function.
NURSING CONSIDERATIONS
PRECAUTIONS
BASELINE ASSESSMENT Contraindications: Hypersensitivity to
Antiemetic: Assess for dehydration (poor me­to­
lazone. Anuria, hepatic coma/pre-
skin turgor, dry mucous membranes, coma. Cautions: History of hypersensitivity
­longitudinal furrows in tongue). Assess to sulfonamides, thiazide diuretics. Severe
for nausea, vomiting, abdominal disten- renal disease, severe hepatic impairment,
tion, bowel sounds. gout, prediabetes or diabetes, elevated
serum cholesterol, triglycerides.

Canadian trade name Non-Crushable Drug High Alert drug


766 metOLazone
ACTION
ADMINISTRATION/HANDLING
Blocks reabsorption of sodium,
PO
potassium, chloride at distal convo-
• May give with food, milk if GI upset
luted tubule, increasing excretion of
occurs, preferably with breakfast (may
sodium, potassium, water. Therapeu-
prevent nocturia).
tic Effect: Reduces B/P, promotes
diuresis. INDICATIONS/ROUTES/DOSAGE
Edema
PHARMACOKINETICS
PO: ADULTS: 2.5–10 mg/day. May
Route Onset Peak Duration increase to 20 mg/day.
PO (diuretic) 1 hr — 24 hrs
Hypertension
Incompletely absorbed from GI PO: ADULTS, ELDERLY: Initially, 2.5–5
tract. Protein binding: 95%. Primar- mg/day. Adjust dose to achieve maximum
ily excreted unchanged in urine. therapeutic effect.
Not removed by hemodialysis. Half-
Dosage in Renal Impairment
life: 20 hrs.
Mild to moderate impairment: No
LIFESPAN CONSIDERATIONS dose adjustment. Severe impairment:
Pregnancy/Lactation: Crosses pla- Use caution.
centa. Small amount distributed in Dosage in Hepatic Impairment
M breast milk. Breastfeeding not recom- No dose adjustment. Contraindicated
mended. Children: No age-related with hepatic coma or precoma.
precautions noted. Elderly: May
be more sensitive to hypotensive or SIDE EFFECTS
electrolyte effects. Age-related renal Expected: Increased urinary frequency/
impairment may require dosage volume. Frequent (10%–9%): Dizziness,
adjustment. light-headedness, headache. Occasional
(6%–4%): Muscle cramps/spasm, drows-
INTERACTIONS iness, fatigue, lethargy. Rare (less than
DRUG: Bile acid sequestrants (e.g., 2%): Asthenia, palpitations, depression,
cholestyramine) may decrease nausea, vomiting, abdominal bloating,
absorption. May increase the hypo- constipation, diarrhea, urticaria.
kalemic effect of topiramate.
HERBAL: Licorice may increase the ADVERSE EFFECTS/TOXIC
hypokalemic effect. Herbals with REACTIONS
hypotensive properties (e.g., Vigorous diuresis may lead to profound
garlic, ginger, ginkgo biloba) water loss and electrolyte depletion, result-
or hypertensive properties ing in hypokalemia, hyponatremia, dehydra-
(e.g., yohimbe) may alter effects. tion. Acute hypotensive episodes may occur.
FOOD: None known. LAB VALUES: May Hyperglycemia may occur during prolonged
increase serum glucose, cholesterol, therapy. Pancreatitis, paresthesia, blood dys-
LDL, bilirubin, calcium, creatinine, crasias, pulmonary edema, allergic pneumo-
uric acid, triglycerides. May decrease nitis, dermatologic reactions occur rarely.
urinary calcium, serum magnesium, Overdose can lead to lethargy, coma without
potassium, sodium. changes in electrolytes, hydration.
AVAILABILITY (Rx) NURSING CONSIDERATIONS
Tablets: 2.5 mg, 5 mg, 10 mg. BASELINE ASSESSMENT
Check vital signs, esp. B/P for hypoten-
sion, before administration. Assess
underlined – top prescribed drug
metoprolol 767
baseline serum electrolytes, particularly uCLASSIFICATION
check for hypokalemia. Assess skin tur- PHARMACOTHERAPEUTIC: Beta 1 -
gor, mucous membranes for hydration adrenergic blocker. CLINICAL: An-
status. Assess for peripheral edema. As- tianginal, antihypertensive, MI ad-
sess muscle strength, mental status. Note junct.
skin temperature, moisture. Obtain base-
line weight. Monitor I&O.
USES
INTERVENTION/EVALUATION
Immediate-Release: Treatment of
Continue to monitor B/P, vital signs, se- hemodynamically stable acute myocardial
rum electrolytes, I&O, weight. Note ex- infarction (AMI) to reduce CV mortality.
tent of diuresis. Monitor for electrolyte Long-term treatment of angina pectoris.
disturbances (hypokalemia may result Management of hypertension. Extended-
in weakness, tremors, muscle cramps, Release: Long-term treatment of angina
nausea, vomiting, altered mental status, pectoris. Management of hypertension.
tachycardia; hyponatremia may result in Treatment of stable symptomatic HF of
confusion, thirst, cold/clammy skin). ischemic, hypertensive, or cardiomyop-
PATIENT/FAMILY TEACHING athic origin to reduce rate of hospitalization
• Expect increased urinary frequency/ in pts receiving ACE inhibitors, diuretics,
volume. • Slowly go from lying to stand- and/or digoxin. Injection: Treatment of
ing to reduce hypotensive effect. • Avoid hemodynamically stable acute myocardial
infarction (AMI) to reduce CV mortal- M
tasks requiring motor skills, mental alert-
ness until response to drug is estab- ity. OFF-LABEL: Treatment of ventricular
lished. • Eat foods high in potassium, arrhythmias, migraine prophylaxis, essen-
such as whole grains (cereals), legumes, tial tremor, aggressive behavior, prevent
meat, bananas, apricots, orange juice, po- reinfarction post-MI, prevent/treat atrial
tatoes (white, sweet), raisins. fibrillation/atrial flutter, hypertrophic car-
diomyopathy, thyrotoxicosis.
PRECAUTIONS
metoprolol Contraindications: Hypersensitivity to
metoprolol. Second- or third-degree
me-toe-pro-lol heart block. Immediate-Release: MI:
(Kaspargo, Lopressor, Toprol XL) Severe sinus bradycardia (HR less than
j BLACK BOX ALERT jAbrupt 45 beats/min), systolic B/P less than 100
withdrawal can produce acute mm Hg, moderate to severe HF, significant
tachycardia, hypertension,
ischemia. Drug should be gradually first-degree heart block. Immediate-
tapered over 1–2 wks. Release: HTN/Angina: Sinus bra-
Do not confuse metoprolol with dycardia, cardiogenic shock, overt HF,
atenolol, labetalol, nadolol, or sick sinus syndrome (except with pace-
stanozolol, or Toprol XL with TE- maker), severe peripheral arterial disease.
Gretol, TEGretol XR, or Topamax. Extended-Release: Severe bradycar-
dia, cardiogenic shock, decompensated
FIXED-COMBINATION(S) HF, sick sinus syndrome (except with
Dutoprol: metoprolol/hydroCHLO- functioning pacemaker). Cautions: Arte-
ROthiazide (a diuretic): 25 mg/12.5 rial obstruction, bronchospastic disease,
mg, 50 mg/12.5 mg, 100 mg/12.5 mg. hepatic impairment, peripheral vascular
Lopressor HCT: metoprolol/hydro- disease, hyperthyroidism, diabetes melli-
chlorothiazide (a diuretic): 50 mg/25 tus, myasthenia gravis, psychiatric disease,
mg, 100 mg/25 mg, 100 mg/50 mg. history of severe anaphylaxis to allergens.
Extended-Release: Compensated HF.
Canadian trade name Non-Crushable Drug High Alert drug
768 metoprolol

ACTION bilirubin, creatinine, potassium, uric acid,


Selectively blocks beta1-adrenergic recep- ALT, AST, triglycerides.
tors. Therapeutic Effect: Slows heart
AVAILABILITY (Rx)
rate, decreases cardiac output, reduces
B/P. Decreases myocardial ischemia Injection Solution: 5 mg/5 mL. Tablets,
severity. Immediate-Release: 25 mg, 37.5 mg, 50
mg, 75 mg, 100 mg.
PHARMACOKINETICS Capsules, Extended-Release Sprin-
Route Onset Peak Duration kle: 25 mg, 50 mg, 100 mg, 200 mg.
PO 10–15 min 1–2 hrs N/A Tablets, Extended-Release: 25 mg, 50
PO N/A 6–12 hrs N/A mg, 100 mg, 200 mg.
(extended-
release) ADMINISTRATION/HANDLING
IV Immediate 20 min N/A
IV
Well absorbed from GI tract. Protein Rate of administration • May give
binding: 12%. Widely distributed. Metab- undiluted. • Administer IV injection
olized in liver. Primarily excreted in over 1 min. • May give by IV piggyback
urine. Removed by hemodialysis. Half- (in 50 mL D5W or 0.9% NaCl) over 30–
life: 3–7 hrs. 60 min. • Monitor ECG, B/P during
LIFESPAN CONSIDERATIONS administration.
M Storage • Store at room temperature.
Pregnancy/Lactation: Crosses pla-
centa; distributed in breast milk. Avoid PO
use during first trimester. May produce • Tablets may be crushed; do not crush
bradycardia, apnea, hypoglycemia, hypo- extended-release tablets. • Extended-re-
thermia during delivery, low-birth-weight lease tablets may be divided in half. • Give
infants. Children: Safety and efficacy at same time each day. • May be given
not established. Elderly: Age-related with or immediately after meals (enhances
peripheral vascular disease may increase absorption). • Sprinkle capsules may be
susceptibility to decreased peripheral given whole or contents may be mixed (1
circulation. teaspoonful) on soft food and used within
60 min.
INTERACTIONS
DRUG: Alpha2 agonists (e.g., cloni- IV INCOMPATIBILITIES
dine) may increase AV-blocking effect. Amphotericin B complex (Abelcet, AmBi-
Strong CYP3A4 inducers (e.g., car- some, Amphotec), lidocaine, nitroglycerin.
BAMazepine, phenytoin, rifAMPin)
may decrease concentration/effect. IV COMPATIBILITIES
Dronedaraone, fingolimod, riv- Amiodarone, dilTIAZem, furosemide,
astigmine may increase bradycardic heparin, morphine.
effect. May increase vasoconstriction
of ergot derivatives (e.g., ergota- INDICATIONS/ROUTES/DOSAGE
mine). HERBAL: Herbals with hyper- Hypertension
tensive properties (e.g., licorice, PO: (Immediate-Release): ADULTS,
yohimbe) or hypotensive properties ELDERLY: Initially, 50 mg twice daily.
(e.g., garlic, ginger, ginkgo biloba) Increase at wkly (or longer) intervals.
may alter effects. FOOD: None known. Usual Range: 100–200 mg/day in 2
LAB VALUES: May increase serum anti- divided doses. Maximum: 450 mg/
nuclear antibody titer (ANA), serum BUN, day. CHILDREN: Initially, 0.5–1 mg/kg/
lipoprotein, LDH, alkaline phosphatase, dose. Maximum Initial Dose: 25 mg.

underlined – top prescribed drug


metoprolol 769
Maximum Daily Dose: 6 mg/kg/day hands/feet. Rare: Altered taste, dry eyes,
or 200 mg/day, whichever is less. nightmares, paresthesia, allergic reac-
PO: (Extended-Release): ADULTS, tion (rash, pruritus).
ELDERLY: Initially, 25–100 mg/day
as single dose. May increase at least ADVERSE EFFECTS/TOXIC
at wkly intervals until optimum B/P REACTIONS
attained. Usual Range: 50–200 mg once Overdose may produce profound bra-
daily. Maximum: 400 mg/day. CHILDREN dycardia, hypotension, bronchospasm.
6 YRS OR OLDER: Initially, 1 mg/kg once Abrupt withdrawal may result in dia-
daily. Maximum Initial Dose: 50 mg. phoresis, palpitations, headache, tremu-
May increase to 2 mg/kg/day or 200 mg/ lousness, exacerbation of angina, MI,
day, whichever is less. ventricular arrhythmias. May precipitate
HF, MI in pts with heart disease, thy-
Angina Pectoris roid storm in those with thyrotoxicosis,
PO: (Immediate-Release): ADULTS: peripheral ischemia in those with exist-
Initially, 50 mg twice daily. Increase at ing peripheral vascular disease. Hypogly-
wkly (or longer) intervals. Usual range: cemia may occur in pts with previously
50–200 mg twice daily. Maximum: 400 controlled diabetes (may mask signs of
mg/day. hypoglycemia). Antidote: Glucagon (see
PO: (Extended-Release): ADULTS: Ini- Appendix J for dosage).
tially, 100 mg/day as single dose. May
increase by at least at wkly intervals until NURSING CONSIDERATIONS M
optimum clinical response achieved.
BASELINE ASSESSMENT
Maximum: 400 mg/day.
Assess baseline renal function, LFT. As-
HF sess B/P, apical pulse immediately before
PO: (Extended-Release): ADULTS: Ini- drug administration (if pulse is 60/min or
tially, 12.5–25 mg/day. May titrate gradu- less or systolic B/P is less than 90 mm Hg,
ally by doubling dose q2wks or longer up withhold medication, contact physician).
to target dose of 200 mg/day. Antianginal: Record onset, type (sharp,
dull, squeezing), radiation, location, in-
Early Treatment of MI tensity, duration of anginal pain, precipi-
IV: ADULTS: 5 mg q5min for up to 3 tating factors (exertion, emotional stress).
doses, followed by 12.5–50 mg q6–12h
in acute setting (begin oral 15–30 min INTERVENTION/EVALUATION
after last IV dose). Transition to meto- Measure B/P near end of dosing inter-
prolol tartrate twice daily or metoprolol val (determines whether B/P is con-
succinate once daily. May increase up to trolled throughout day). Monitor B/P
a maximum of 200 mg/day. for hypotension, respiration for short-
ness of breath. Assess pulse for qual-
Dosage in Renal/Hepatic Impairment ity, rate, rhythm. Assess for evidence
No dose adjustment. of HF: dyspnea (esp. on exertion, lying
down), night cough, peripheral edema,
SIDE EFFECTS distended neck veins. Monitor I&O (in-
Metoprolol is generally well tolerated, creased weight, decreased urinary output
with transient and mild side effects. may indicate HF). Therapeutic response
Frequent: Diminished sexual function, to hypertension noted in 1–2 wks.
drowsiness, insomnia, unusual fatigue/
weakness. Occasional: Anxiety, diar- PATIENT/FAMILY TEACHING
rhea, constipation, nausea, vomiting, • Do not abruptly discontinue medica-
nasal congestion, abdominal discom- tion. • Compliance with therapy regimen
fort, dizziness, difficulty breathing, cold is essential to control hypertension,
Canadian trade name Non-Crushable Drug High Alert drug
770 metroNIDAZOLE
arrhythmias. • If dose is missed, take next PRECAUTIONS
scheduled dose (do not double Contraindications: Hypersensitivity to
dose). • Go from lying to standing metronidazole. Pregnancy (first trimes-
slowly. • Report excessive fatigue, dizzi- ter with trichomoniasis), use of disulfi-
ness. • Avoid tasks that require alertness, ram within 2 wks, use of alcohol during
motor skills until response to drug is estab- therapy or within 3 days of discontinuing
lished. • Do not use nasal decongestants, metroNIDAZOLE. Cautions: Blood dys-
OTC cold preparations (stimulants) without crasias, severe hepatic dysfunction, end-
physician approval. • Monitor B/P, pulse stage renal disease, seizure disorder, HF,
before taking medication. • Restrict salt, other sodium-retaining states, elderly.
alcohol intake.
ACTION
Diffuses into organism, interacting with
DNA causing a loss of helical DNA structure
metroNIDAZOLE and strand breakage, inhibiting protein
synthesis. Therapeutic Effect: Produces
me-troe-nye-da-zole bactericidal, antiprotozoal, amebicidal,
(Flagyl, MetroCream, MetroGel, trichomonacidal effects. Produces anti-
MetroGel-Vaginal, NidaGel , inflammatory, immunosuppressive effects
Noritate, Vandazole) when applied topically.
Do not confuse metroNIDAZOLE
M with meropenem, metFORMIN, PHARMACOKINETICS
methotrexate, or miconazole. Well absorbed from GI tract; minimally
absorbed after topical application.
FIXED-COMBINATION(S)
Protein binding: less than 20%. Widely
Helidac: metronidazole/bismuth/ distributed; crosses blood-brain bar-
tetracycline (an anti-infective): 250 rier. Metabolized in liver. Excreted in
mg/262 mg/500 mg. Pylera: metroNI- urine (80%), feces (15%). Removed
DAZOLE/bismuth/tetracycline (an anti- by hemodialysis. Half-life: 8 hrs
infective): 125 mg/140 mg/125 mg. (increased in cirrhosis, neonates).
uCLASSIFICATION
Active metabolite prolonged in renal
failure.
PHARMACOTHERAPEUTIC: Nitro-
imidazole derivative. CLINICAL: An- LIFESPAN CONSIDERATIONS
tibacterial, antiprotozoal, amebicide. Pregnancy/Lactation: Readily crosses
placenta. Distributed in breast milk.
USES Contraindicated during first trimester in
those with trichomoniasis. Topical use
Systemic: Treatment of anaerobic infec- during pregnancy, lactation discour-
tions (skin/skin structure, CNS, lower aged. Children: Safety and efficacy of
respiratory tract, bone/joints, intra- topical administration not established in
abdominal, gynecologic, endocarditis, pts younger than 21 yrs. Elderly: Age-
septicemia). Treatment of H. pylori (part related hepatic impairment may require
of multidrug regimen); surgical prophy- dosage adjustment.
laxis (colorectal), trichomoniasis, ame-
biasis. Topical treatment of acne rosacea INTERACTIONS
or inflammatory lesions. Vaginal gel: DRUG: Alcohol may cause disulfiram-
Treatment of bacterial vaginosis. OFF- type reaction (e.g., abdominal cramps,
LABEL: Crohn’s disease, urethritis. Anti- nausea, vomiting, headache, psychotic
biotic-associated pseudomembranous reactions). Disulfiram may increase
colitis (AAPC) caused by C. difficile. risk of toxicity. May increase effects of
underlined – top prescribed drug
metroNIDAZOLE 771
oral anticoagulants (e.g., warfarin). IV: CHILDREN, INFANTS: 22.5–40 mg/
HERBAL: None significant. FOOD: None kg/day in 3 divided doses. Maximum:
known. LAB VALUES: May increase 1,500 mg/day.
serum LDH, ALT, AST.
Intra-abdominal Infections
AVAILABILITY (Rx) IV: ADULTS, ELDERLY: 500 mg q6h. Max-
Capsules: 375 mg. Injection, Infusion: 500 imum: 4 g/day. CHILDREN: 30–40 mg/
mg/100 mL. Tablets: (Flagyl): 250 mg, kg/day in 3 divided doses. Maximum
500 mg. Topical Cream: (MetroCream): dose: 500 mg/dose.
0.75% (Noritate): 1%. Topical Gel: (Metro- Pseudomembranous Colitis
Gel): 0.75%, 1%. Vaginal Gel: (MetroGel- PO: ADULTS, ELDERLY: 250–500 mg 3–4
Vaginal, Vandazole): 0.75%. times/day. CHILDREN: 30 mg/kg/day in
ADMINISTRATION/HANDLING divided doses q6h for 7–10 days. Maxi-
mum: 2 g/day.
IV
Bacterial Vaginosis
Rate of administration • Infuse IV Intravaginal: ADULTS: 0.75% apply 1–2
over 30–60 min. Do not give by IV bolus. times/day for 5 days. 1.3% apply once as
Storage • Store at room tempera- a single dose. PO: 500 mg twice daily for
ture (ready-to-use infusion bags). 7 days.

PO b ALERT c Centers for Disease Control M


• Give without regard to food. Give and Prevention (CDC) does not recommend
with food to decrease GI irritation. the use of topical agents during pregnancy.

IV INCOMPATIBILITIES Rosacea
Amphotericin B complex (Abelcet, AmBi- Topical: ADULTS, ELDERLY: (1%): Apply
some, Amphotec). to affected area once daily. (0.75%): Apply
to affected area twice daily.
IV COMPATIBILITIES Dosage in Renal Impairment
Dexmedetomidine (Precedex), dilTIA- No dose adjustment.
Zem (Cardizem), DOPamine (Intro-
pin), heparin, HYDROmorphone Dosage in Hepatic Impairment
(Dilaudid), LORazepam (Ativan), mag- Mild to moderate impairment: Use
nesium sulfate, midazolam (Versed), caution. No dose adjustment. Severe
morphine. impairment: Reduce dose by 50% for
immediate-release; not recommended
INDICATIONS/ROUTES/DOSAGE for extended-release.
Amebiasis
PO: ADULTS, ELDERLY: (Immediate- SIDE EFFECTS
Release): 500–750 mg q8h for 7–10 Frequent: Systemic: Anorexia, nausea,
days. CHILDREN: 35–50 mg/kg/day in dry mouth, metallic taste. Vaginal: Symp-
divided doses q8h for 7–10 days. tomatic cervicitis/vaginitis, abdominal
cramps, uterine pain. Occasional: Sys-
Anaerobic Infections temic: Diarrhea, constipation, vomiting,
PO, IV: ADULTS, ELDERLY: 500 mg q6–8h. dizziness, erythematous rash, urticaria,
Maximum: 4 g/day. reddish-brown urine. Topical: Tran-
PO: CHILDREN, INFANTS: 30–50 mg/ sient erythema, mild dryness, burning,
kg/day in divided doses q8h. Maxi- irritation, stinging, tearing when applied
mum: 2,250 mg/day. too close to eyes. Vaginal: Vaginal,

Canadian trade name Non-Crushable Drug High Alert drug


772 micafungin
perineal, vulvar itching; vulvar swelling. giectasia, ocular problems (conjunctivitis,
Rare: Mild, transient leukopenia; throm- keratitis, blepharitis). • Other recom-
bophlebitis with IV therapy. mendations for rosacea include avoidance
of hot/spicy foods, alcohol, extremes of
ADVERSE EFFECTS/TOXIC hot/cold temperatures, excessive sunlight.
REACTIONS
Oral therapy may result in furry tongue,
glossitis, cystitis, dysuria, pancreatitis.
Peripheral neuropathy (manifested as micafungin
numbness, tingling of hands/feet) usually
is reversible if treatment is stopped imme- mye-ka-fun-jin
diately upon appearance of neurologic (Mycamine)
symptoms. Seizures occur occasionally.
uCLASSIFICATION
NURSING CONSIDERATIONS PHARMACOTHERAPEUTIC: Echino-
BASELINE ASSESSMENT candin antifungal. CLINICAL: Anti-
fungal.
Obtain baseline CBC, LFT. Question for
history of hypersensitivity to metroni-
dazole, other nitroimidazole derivatives USES
(and parabens with topical). Obtain Treatment of esophageal candidiasis, can-
M specimens for diagnostic tests, cultures didemia, candida peritonitis, abscesses,
before giving first dose (therapy may be- acute disseminated candidiasis, prophy-
gin before results are known). laxis of Candida infection in pts under-
INTERVENTION/EVALUATION going hematopoietic stem cell transplant.
OFF-LABEL: Treatment of infections due to
Monitor daily pattern of bowel activity,
stool consistency. Monitor I&O, assess Aspergillus spp.
for urinary problems. Be alert to neuro- PRECAUTIONS
logic symptoms (dizziness, paresthesia of
Contraindications: Hypersensitivity to
extremities). Assess for rash, urticaria.
Monitor for onset of superinfection (ul- micafungin. Cautions: Hepatic/renal impair­
ceration/change of oral mucosa, furry ment, concomitant hepatotoxic medi­cations.
tongue, vaginal discharge, genital/anal ACTION
pruritus).
Inhibits synthesis of glucan (vital com-
PATIENT/FAMILY TEACHING ponent of fungal cell formation), damag-
• Urine may be red-brown or dark. ing fungal cell membrane. Therapeutic
• Avoid alcohol, alcohol-containing prepa- Effect: Decreased glucan content leads
rations (cough syrups, elixirs) for at least to cellular lysis.
48 hrs after last dose. • Avoid tasks that
require alertness, motor skills until re- PHARMACOKINETICS
sponse to drug is established. • If taking Slowly metabolized in liver. Protein bind-
metroNIDAZOLE for trichomoniasis, refrain ing: greater than 99%. Primarily excreted
from sexual intercourse until full treatment in feces. Not removed by hemodialysis.
is completed. • For amebiasis, frequent Half-life: 11–21 hrs.
stool specimen checks will be neces-
sary. • Topical: Avoid contact with LIFESPAN CONSIDERATIONS
eyes. • May apply cosmetics after applica- Pregnancy/Lactation: May reduce
tion. • Metronidazole acts on erythema, sperm count. May be embryotoxic.
papules, pustules but has no effect on Unknown if distributed in breast milk.
­rhinophyma (hypertrophy of nose), telan- Children: Safety and efficacy not

underlined – top prescribed drug


micafungin 773
established. Elderly: No age-related Candida Prophylaxis in Stem Cell Pts
precautions noted. IV: ADULTS, ELDERLY: 50 mg/day. CHIL-
DREN 4 MOS OR OLDER: 1 mg/kg/day.
INTERACTIONS Maximum: 50 mg/day.
DRUG: May decrease therapeutic effect
of Saccharomyces boulardii. May Candidemia, Disseminated Candidiasis,
increase concentration/effect of siro- Peritonitis, Abscesses
limus. HERBAL: None significant. IV: ADULTS, ELDERLY: 100 mg/day for 15
FOOD: None known. LAB VALUES: May days. CHILDREN 4 MOS OR OLDER: 2 mg/
increase serum creatinine, alkaline phos- kg/day. Maximum: 100 mg daily.
phatase, LDH, ALT, AST. Dosage in Renal/Hepatic Impairment
AVAILABILITY (Rx) No dose adjustment.
Injection, Powder for Reconstitution: 50 SIDE EFFECTS
mg, 100 mg. Occasional (3%–2%): Nausea, headache,
ADMINISTRATION/HANDLING diarrhea, vomiting, fever. Rare (1%): Diz-
ziness, drowsiness, pruritus, abdominal
IV pain, dyspepsia.
Reconstitution • Add 5 mL 0.9%
NaCl (without bacteriostatic agent) to ADVERSE EFFECTS/TOXIC
each 50-mg vial (10 mL to 100-mg vial) REACTIONS
M
to yield micafungin 10 mg/mL. • Gently Hypersensitivity reaction character-
swirl to dissolve; do not shake. • Fur- ized by rash, pruritus, facial edema
ther dilute in 0.9% NaCl or D5W to final occurs rarely. Anaphylaxis, hemoglo-
concentration of 0.5–1.5 mg/mL. • Al- binuria, hemolytic anemia have been
ternatively, D5W may be used for recon- reported.
stitution and dilution. • Flush existing
IV line with 0.9% NaCl or D5W before NURSING CONSIDERATIONS
infusion. BASELINE ASSESSMENT
Rate of administration • Infuse over Determine baseline renal function, LFT
60 min. and periodically thereafter.
Storage • Reconstituted solution is
stable for 24 hrs at room tempera- INTERVENTION/EVALUATION
ture. • Discard if precipitate is present. Monitor BUN, serum creatinine, CrCl,
LFT. Monitor for hepatotoxicity.
IV INCOMPATIBILITIES
Amiodarone, nicardipine. PATIENT/FAMILY TEACHING
• Report liver problems such as bruis-
IV COMPATIBILITIES ing, confusion; dark amber or orange-
Bumetanide (Bumex), calcium gluco- colored urine; right upper abdominal
nate, heparin. pain; yellowing of the skin or eyes. • Re-
port decreased urine output; dark, am-
INDICATIONS/ROUTES/DOSAGE ber urine; swelling of the hands or
Esophageal Candidiasis feet. • Do not take OTC medications
IV: ADULTS, ELDERLY: 150 mg/day for that are toxic to the liver (e.g., acet-
10–30 days. CHILDREN 4 MOS OR OLDER aminophen).
WEIGHING MORE THAN 30 KG: 2.5 mg/kg/
day. Ma­ximum: 150 mg daily. 30 KG OR
LESS: 3 mg/kg/day.

Canadian trade name Non-Crushable Drug High Alert drug


774 midazolam

PHARMACOKINETICS
midazolam Route Onset Peak Duration
mye-da-zoe-lam PO 10–20 min N/A N/A
IV 1–5 min 5–7 min 20–30 min
(Nayzilam) IM 5–15 min 30–60 min 2–6 hrs
j BLACK BOX ALERT jMay
cause severe respiratory depres- Well absorbed after IM administration.
sion, respiratory arrest, apnea. Protein binding: 97%. Metabolized in liver.
Initial doses in elderly should be
conservative. Do not administer by Primarily excreted in urine. Not removed
rapid IV injection in neonates (may by hemodialysis. Half-life: 1–5 hrs.
cause severe hypotension/sei-
zures). Use with opioids may cause LIFESPAN CONSIDERATIONS
profound sedation, respiratory Pregnancy/Lactation: Crosses pla-
depression, coma, or death.
centa. Unknown if drug is distributed in
Do not confuse midazolam with, breast milk. Children: Neonates more
ALPRAZolam or LORazepam. likely to have respiratory depression.
uCLASSIFICATION Elderly: Age-related renal impairment
may require dosage adjustment.
PHARMACOTHERAPEUTIC: Ben-
zodiazepine (Schedule IV). CLINI- INTERACTIONS
CAL: Sedative, anxiolytic.
DRUG: Alcohol, other CNS depres-
M sants (e.g., LORazepam, morphine,
USES zolpidem) may increase CNS effects,
respiratory depression, hypotensive effect.
Sedation, anxiolytic, amnesia before proce-
Strong CYP3A4 inhibitors (e.g., clar-
dure or induction of anesthesia, conscious
ithromycin, ketoconazole, ritona-
sedation before diagnostic/radiographic
vir) may increase concentration/effect.
procedure, continuous IV sedation of
Strong CYP3A4 inducers (e.g., car-
intubated or mechanically ventilated pts.
BAMazepine, phenytoin, rifAMPin)
Nasal: Acute treatment of seizure clusters.
may decrease concentration/effect.
OFF-LABEL: Anxiety, status epilepticus, con-
HERBAL: Herbals with sedative prop-
scious sedation (intranasal route).
erties (e.g., chamomile, kava kava,
PRECAUTIONS valerian) may increase CNS depression.
St. John’s wort may decrease concen-
Contraindications: Hypersensitiv-
tration. FOOD: Grapefruit products
ity to midazolam. Acute narrow-angle
increase oral absorption, systemic avail-
glaucoma, concurrent use of protease
ability. LAB VALUES: None significant.
inhibitors (e.g., atazanavir, darunavir).
Cautions: Renal/hepatic/pulmonary AVAILABILITY (Rx)
impairment, impaired gag reflex, HF,
Injection Solution: 1 mg/mL, 5 mg/mL.
treated open-angle glaucoma, obese pts,
Nasal Spray: 5 mg/0.1 ml. Syrup: 2 mg/mL.
concurrent CNS depressants, ­ alcohol
dependency, elderly pts, debilitated pts. ADMINISTRATION/HANDLING
ACTION IV
Enhances action of gamma-aminobutyric Rate of administration
acid (GABA), one of the major inhibitory • May give undiluted or as infusion.
neurotransmitters in the brain. Thera- • Resuscitative equipment, O2 must be
peutic Effect: Produces anxiolytic, hyp- readily available before IV administra-
notic, anticonvulsant, muscle relaxant, tion. • Administer by slow IV injection
amnestic effects. over at least 2–5 min at concentration of

underlined – top prescribed drug


midazolam 775
1–5 mg/mL. • Reduce IV rate in those effect. Usual range: 0.4–9.4 mcg/kg/min.
older than 60 yrs, debilitated pts with
chronic disease states, pulmonary im- Seizure Clusters
pairment. • Too-rapid IV rate, exces- Nasal: ADULTS, CHILDREN 12 YRS AND
sive doses, or single large dose increases OLDER: Initially, one spray (5-mg dose)
risk of respiratory depression/arrest. into one nostril. One additional spray
Storage • Store vials at room temper- (5-mg dose) into the opposite nostril
ature. may be administered after 10 min.
Maximum dose: 10 mg (2 sprays)
IM per episode. Maximum frequency:
• Give deep IM into large muscle mass. 1 episode q3days; 5 episodes/mos.
Maximum concentration: 1 mg/mL.
Dosage in Renal Impairment
PO No dose adjustment.
• Do not mix with grapefruit juice.
Dosage in Hepatic Impairment
IV INCOMPATIBILITIES Use caution.
Albumin, amphotericin B complex (Abelcet,
AmBisome, Amphotec), ampicillin (Polycil- SIDE EFFECTS
lin), ampicillin and sulbactam (Unasyn), Frequent (10%–4%): Decreased respira-
bumetanide (Bumex), co-trimoxazole tory rate, tenderness at IM or IV injec-
(Bactrim), dexamethasone (Decadron), tion site, pain during injection, oxygen
fosphenytoin (Cerebyx), furosemide (Lasix), desaturation, hiccups. Occasional (3%– M
hydrocortisone (Solu-Cortef), methotrexate, 2%): Hypotension, paradoxical CNS
nafcillin (Nafcil), sodium bicarbonate. reaction. Rare (less than 2%): Nausea,
vomiting, headache, coughing.
IV COMPATIBILITIES
ADVERSE EFFECTS/TOXIC
Amiodarone (Cordarone), atropine, REACTIONS
calcium gluconate, dexmedetomidine
(Precedex), dilTIAZem (Cardizem), Inadequate or excessive dosage,
diphenhydrAMINE (Benadryl), DOBUTa- improper administration may result in
mine (Dobutrex), DOPamine (Intropin), cerebral hypoxia, agitation, involuntary
etomidate (Amidate), fentaNYL (Subli- movements, hyperactivity, combativeness.
maze), glycopyrrolate (Robinul), heparin, Too-rapid IV rate, excessive doses, or
HYDROmorphone (Dilaudid), hydrOXY- single large dose increases risk of respi-
zine (Vistaril), insulin, LORazepam (Ati- ratory depression/arrest. Respiratory
van), milrinone (Primacor), morphine, depression/apnea may produce hypoxia,
nitroglycerin, norepinephrine (Levophed), cardiac arrest.
potassium chloride, propofol (Diprivan). NURSING CONSIDERATIONS
INDICATIONS/ROUTES/DOSAGE BASELINE ASSESSMENT
Continuous Sedation During Mechanical Resuscitative equipment, oxygen must be
Ventilation available. Obtain vital signs before admin-
IV: ADULTS, ELDERLY: Initially, 0.01–0.05 istration. Assess level of consciousness.
mg/kg (1–5 mg in 70-kg adult). May
repeat at 5- to 15-min intervals until ade- INTERVENTION/EVALUATION
quate sedation achieved or continuous Monitor respiratory rate, oxygen saturation
infusion rate of 0.02–0.1 mg/kg/hr and continuously during parenteral administra-
titrated to desired effect. CHILDREN: Ini- tion for underventilation, apnea. Monitor
tially, 0.05–0.2 mg/kg followed by con- vital signs, level of sedation q3–5min during
tinuous infusion of 0.06–0.12 mg/kg/hr recovery period. Assess level of conscious-
(1–2 mcg/kg/min) titrated to desired ness for effectiveness.
Canadian trade name Non-Crushable Drug High Alert drug
776 midodrine
systemic circulation. Excreted in urine.
midodrine Half-life: 0.5 hr.
mye-doe-dreen LIFESPAN CONSIDERATIONS
(Amatine , Apo-Midodrine ) Pregnancy/Lactation: Unknown if
j BLACK BOX ALERT j Can drug crosses placenta or is distributed
cause marked rise in supine blood in breast milk. Children: Safety and
pressure; use in pts for whom or-
thostatic hypotension significantly efficacy not established. Elderly: Age-
impairs daily life. related renal impairment may require
Do not confuse Amatine with dosage adjustment.
amantadine or protamine, or
midodrine with Midrin. INTERACTIONS
DRUG: Ergot derivatives (e.g.,
uCLASSIFICATION ergotamine), linezolid, MAOIs (e.g.,
PHARMACOTHERAPEUTIC: Alpha 1 phenelzine, selegiline) may increase
agonist. CLINICAL: Vasopressor. hypertensive effects. HERBAL: None sig-
nificant. FOOD: None known. LAB VAL-
UES: None significant.
USES
Treatment of symptomatic orthostatic AVAILABILITY (Rx)
hypotension. OFF-LABEL: Vasovagal syn- Tablets: 2.5 mg, 5 mg, 10 mg.
M cope, prevention of dialysis-induced
hypotension. ADMINISTRATION/HANDLING
• Give without regard to food. • Last
PRECAUTIONS dose of day should be given 3–4 hrs be-
Contraindications: Hypersensitivity to fore bedtime.
midodrine. Acute renal failure, persistent
supine hypertension, pheochromocytoma, INDICATIONS/ROUTES/DOSAGE
severe cardiac disease, thyrotoxicosis, uri- Orthostatic Hypotension
nary retention. Cautions: Renal/hepatic PO: ADULTS, ELDERLY: 2.5–10 mg 3
impairment, history of visual problems, times/day (q3–4hrs). Give during the day
diabetes, immobility, pts who are unable when pt is upright, such as upon aris-
to stand. Concurrent administration with ing, midday, and late afternoon. Do not
digoxin, beta blockers (e.g., metoprolol), give less than 4h before bedtime. Maxi-
vasoconstrictors (e.g., norepinephrine). mum: 40 mg/day.

ACTION Dosage in Renal Impairment


2.5 mg 3 times/day; increase gradually,
Forms active metabolite desglymido- as tolerated. Hemodialysis: Dose after
drine, an alpha1 agonist, increasing arte- HD unless used to prevent HD-induced
riolar and venous tone. Therapeutic hypotension.
Effect: Increases standing, sitting, and
supine systolic B/P in pts with orthostatic Dosage in Hepatic Impairment
hypotension. Use caution.
PHARMACOKINETICS SIDE EFFECTS
Route Onset Peak Duration Frequent (20%–7%): Paresthesia, pilo-
PO 1 hr — 2–3 hrs erection, pruritus, dysuria, supine hyper-
tension. Occasional (6%–1%): Pain, rash,
Rapid absorption from GI tract follow- chills, headache, facial flushing, confu-
ing PO administration. Protein binding: sion, dry mouth, anxiety.
Low. Undergoes enzymatic hydrolysis in

underlined – top prescribed drug


midostaurin 777

ADVERSE EFFECTS/TOXIC neoplasm (SM-AHN), or mast cell leuke-


REACTIONS mia (MCL).
May cause marked increase of supine
PRECAUTIONS
systolic BP (supine hypertension).
Contraindications: Hypersensitivity to
NURSING CONSIDERATIONS midostaurin. Cautions: Baseline anemia,
leukopenia, neutropenia, thrombocyto-
BASELINE ASSESSMENT penia; concomitant use of strong CYP3A
Assess sensitivity to midodrine, other inhibitors, strong CYP3A inducers; pts at
medications (esp. digoxin, sodium-re- risk for hemorrhage (e.g., history of GI
taining vasoconstrictors). Assess medical bleeding, coagulation disorders, recent
history, esp. for renal impairment, severe trauma; concomitant use of anticoagu-
hypertension, cardiac disease. lants, NSAIDs, antiplatelet medication).
INTERVENTION/EVALUATION ACTION
Monitor B/P, renal, hepatic, cardiac Inhibits multiple receptors including
function. FLT3 receptor signaling, and cell prolif-
PATIENT/FAMILY TEACHING eration. Therapeutic Effect: Induces
• Do not take last dose of the day after apoptosis in ITD and ITD mutant express-
evening meal or less than 4 hrs before ing leukemic cells.
bedtime. • Do not give if pt will be su- PHARMACOKINETICS
pine. • Use caution with OTC medica- M
tions that may affect B/P (e.g., cough and Widely distributed. Metabolized in liver.
cold, diet medications). Protein binding: 99.8%. Peak plasma
concentration: 1–3 hrs. Steady state
reached in 28 days. Excreted in feces
(95%), urine (5%). Half-life: 21 hrs.
midostaurin LIFESPAN CONSIDERATIONS
mye-doe-staw-rim Pregnancy/Lactation: Avoid pregnancy;
(Rydapt) may cause fetal harm. Females of repro-
Do not confuse midostaurin ductive potential and males with female
with midodrine. partners of reproductive potential should
use effective contraception during treat-
uCLASSIFICATION ment and for at least 4 mos after discon-
PHARMACOTHERAPEUTIC: FLT inhib- tinuation. Unknown if distributed in breast
itor. Tyrosine kinase inhibitor. CLINI- milk. Breastfeeding not recommended.
CAL: Antineoplastic. May impair fertility in both females and
males. Children: Safety and efficacy not
established. Elderly: No age-related pre-
USES cautions noted.
Treatment of adult pts with newly diag-
nosed acute myeloid leukemia (AML) INTERACTIONS
who are FLT3 mutation–positive, as DRUG: Moderate CYP3A4 inhibitors
detected by an FDA-approved test (in (e.g., ciprofloxacin, fluconazole,
combination with standard cytarabine verapamil), strong CYP3A4 inhibi-
and daunorubicin induction and cyta- tors (e.g., clarithromycin, keto-
rabine consolidation chemotherapy). conazole, ritonavir) may increase
Treatment of adult pts with aggressive concentration/effect. Strong CYP3A4
systemic mastocytosis (ASM), systemic inducers (e.g., carBAMazepine,
mastocytosis with associated hematologic phenytoin, rifAMPin) may decrease

Canadian trade name Non-Crushable Drug High Alert drug


778 midostaurin
concentration/effect. QT-prolonging daily if 50 mg dose is tolerated. If treatment-
agents (e.g., amiodarone, halo- induced neutropenia persists for more than
peridol, moxifloxacin, sotalol) 21 days, permanently discontinue.
may enhance QT-prolonging effect.
May decrease therapeutic effect of BCG. Thrombocytopenia
HERBAL: St. John’s wort may decrease Platelet count less than 50,000 cells/
concentration/effect. FOOD: Grape- mm3 (treatment-induced) in pts
fruit products may increase concen- without MCL; platelet count less
tration/effect. LAB VALUES: May increase than 25,000 cells/mm3 (treatment-
serum alkaline phosphatase, ALT, AST, induced) in pts with baseline platelet
bilirubin, creatinine, GGT, glucose, count 25,000–75,000 cells/mm3: With-
lipase, sodium, uric acid. May decrease hold treatment until platelet count greater
Hgb, Hct, lymphocytes, leukocytes, neu- than or equal to 50,000 cells/mm3, then
trophils, platelets, RBCs; serum albumin, resume at 50 mg twice daily. May increase
magnesium, phosphate, potassium. May to 100 mg twice daily if 50-mg dose is
increase or decrease serum calcium or tolerated. If treatment-induced thrombo-
sodium. May prolong aPTT. cytopenia persists for more than 21 days,
permanently discontinue.
AVAILABILITY (Rx)
Anemia
Capsules: 25 mg.
Hgb less than 8 g/dL (treatment-
M ADMINISTRATION/HANDLING induced) in pts without MCL; life-
threatening anemia with baseline
PO
Hgb 8–10 g/dL (treatment-induced):
• Give with food. • Administer whole;
do not cut, crush, open capsules. Withhold treatment until Hgb greater than
or equal to 8 g/dL, then resume at 50 mg
INDICATIONS/ROUTES/DOSAGE twice daily. May increase to 100 mg twice
Acute Myeloid Leukemia (FLT positive)
daily if 50-mg dose is tolerated. If treat-
PO: ADULTS, ELDERLY: 50 mg twice daily
ment-induced anemia persists for more
(at 12-hr intervals) on days 8–21 of each than 21 days, permanently discontinue.
induction in combination with cytarabine Nausea, Vomiting
and daunorubicin, and on days 8–21 of CTCAE Grade 3 or 4 nausea, vomit-
each cycle of consolidation with high-dose ing despite antiemetic therapy: With-
in combination with cytarabine. hold treatment for 3 days (6 doses), then
Systemic Mastocytosis, Mast Cell resume at 50 mg twice daily. May increase
Leukemia to 100 mg twice daily if 50-mg dose is
PO: ADULTS, ELDERLY: 100 mg twice tolerated.
daily. Continue until disease progression Nonhematologic Toxicities
or unacceptable toxicity. Any other grade toxicities: Withhold
DOSE MODIFICATION FOR SYSTEMIC treatment until resolved to CTCAE Grade
MASTOCYTOSIS 2 or less, then resume at 50 mg twice
Neutropenia daily. May increase to 100 mg twice daily
Treatment-induced ANC less than if 50-mg dose is tolerated.
1,000 cells/mm3 in pts without MCL;
Dosage in Rena/Hepatic Impairment
treatment-induced ANC less than
500 cells/mm3 in pts with baseline
Not specified; use caution.
ANC 500–1,500 cells/mm3: Withhold SIDE EFFECTS
treatment until ANC greater than or equal
to 1,000 cells/mm3, then resume at 50-mg AML: Frequent (83%–24%): Nausea, muco-
twice daily. May increase to 100 mg twice sitis, stomatitis, laryngeal pain, vomiting,

underlined – top prescribed drug


midostaurin 779
headache, petechiae, musculoskeletal pain. Screen for active infection. To reduce
Occasional (20%–7%): Hyperglycemia, risk of nausea/vomiting, administer an-
hemorrhoids, arthralgia, hyperhidrosis, tiemetic before treatment. Obtain ECG in
insomnia, hypertension, dry skin, increased pts taking QT interval–prolonging medi-
weight. Rare (4%–3%): Tremor, eyelid cations. Receive full medication history
edema. Systemic mastocytosis: Frequent and screen for interactions. Question
(82%–23%): Nausea, vomiting, diarrhea, history as listed in Precautions. Question
edema, peripheral edema, fatigue, asthenia, plans of breastfeeding. Confirm compli-
musculoskeletal pain, back pain, extremity ance of effective contraception. Offer
pain, abdominal pain, constipation, pyrexia, emotional support.
headache, dyspnea, bronchospasm. Occa-
sional (19%–6%): Arthralgia, cough, rash, INTERVENTION/EVALUATION
dizziness, insomnia, hypotension, dyspep- Monitor ANC, CBC for anemia, leukope-
sia. Rare (5%–4%): Vertigo, chills, mental nia, neutropenia, lymphopenia, throm-
status change. bocytopenia. Monitor BMP for renal
insufficiency, electrolyte imbalance (esp.
ADVERSE EFFECTS/TOXIC in pts with diarrhea, vomiting, malnu-
REACTIONS trition); LFT for transaminitis, hepato-
Anemia, leukopenia, lymphopenia, neu- toxicity. Diligently screen for infections,
tropenia, thrombocytopenia are expected sepsis; provide appropriate antimicrobial
responses to therapy. Hypersensitivity therapy if indicated. Obtain ABG, radio-
reactions including anaphylaxis, angio- logic test if interstitial lung disease or M
edema, dyspnea, itching, flushing may pneumonitis suspected. Monitor for tox-
occur. Infections including bronchitis, icities at least wkly for 4 wks, then every
bronchopulmonary aspergillosis, colitis, other wk for 8 wks, then monthly there-
cellulitis, device-related infection, erysip- after. If treatment-related toxicities occur,
elas, fungal pneumonia, gastroenteritis, consider referral to specialist. Monitor
hepatic candidiasis, herpes zoster, naso- for hemorrhage, melena, hematuria;
pharyngitis, oral herpes, pneumonia, hypersensitivity reactions; myocardial in-
sepsis, sinusitis, splenic fungal infection, farction, pulmonary disease, thrombosis.
upper respiratory tract infection, urinary Monitor I&O.
tract infection have occurred. Renal fail-
PATIENT/FAMILY TEACHING
ure, acute kidney injury may occur. Other
adverse effects including angina pectoris, • Blood levels will be routinely moni-
cardiac failure, contusion, duodenal ulcer tored. • Treatment may depress your
hemorrhage, epistaxis, gastritis, febrile immune system and reduce your ability
neutropenia, GI bleeding, hematoma, to fight infection. Report symptoms of
interstitial lung disease, myocardial infarc- infection such as body aches, burning
tion, myocardial ischemia, pericardial with urination, chills, cough, fatigue, fe-
effusion, pneumonitis, pulmonary conges- ver. Avoid those with active infection.
tion, pulmonary edema, thrombosis were • Report symptoms of kidney failure
reported. May prolong QT interval. (decreased urination, amber-colored
urine, flank pain, fatigue, swelling of the
NURSING CONSIDERATIONS hands or feet); liver problems (bruising,
confusion; amber, dark, orange-colored
BASELINE ASSESSMENT urine; right upper abdominal pain, yel-
Obtain ANC, CBC, BMP, LFT; serum mag- lowing of the skin or eyes); lung prob-
nesium; vital signs. Ensure electrolytes lems (severe cough, difficulty breathing,
are corrected prior to initiation. In fe- lung pain, shortness of breath). • Avoid
males of reproductive potential, obtain pregnancy. Females and males of child-
pregnancy test within 7 days of initiation. bearing potential should use effective

Canadian trade name Non-Crushable Drug High Alert drug


780 milnacipran
contraception during treatment and for in pts receiving linezolid or IV methylene
at least 4 mos after last dose. Do not blue. Cautions: Pts with depression, pts at
breastfeed. • Treatment may impair increased risk of suicide, other psychiatric
fertility. • Avoid grapefruit products, disorders; elevated blood pressure or heart
Seville oranges, starfruit, herbal supple- rate, seizure disorder, pts with substantial
ments. • Do not take newly prescribed alcohol use or chronic hepatic disease,
medications unless approved by the pre- pts with history of dysuria (e.g., prostatic
scriber who originally started treat- hypertrophy, prostatitis), controlled nar-
ment. • Heart attacks have occurred; row-angle glaucoma, renal impairment,
immediately report chest pain, sweating, cardiovascular disease, elderly.
fainting, palpitations, jaw pain, pain that
radiates to the left arm. • Antinausea ACTION
medication will be given before treatment Appears to inhibit serotonin and norepineph-
to reduce the risk of nausea or vomit- rine reuptake at CNS neuronal presynaptic
ing. • Report bleeding of any kind, esp. membranes. Therapeutic Effect: Reduces
nosebleeds, blood in stool or urine. chronic pain, fatigue, depression, sleep
• Allergic reactions such as anaphylaxis, disorders associated with fibromyalgia syn-
difficulty breathing, itching, flushing, drome; improves physical function.
rash may occur.
PHARMACOKINETICS
Well absorbed following PO administration.
M Protein binding: 13%. Excreted unchanged
milnacipran in urine. Steady-state levels reached in
36–48 hrs. Half-life: 6–8 hrs.
mil-nay-sip-ran
(Savella) LIFESPAN CONSIDERATIONS
j BLACK BOX ALERT jIncreased Pregnancy/Lactation: Increased risk
risk of suicidal ideation and of fetal complications, including need
behavior in children, adolescents, for respiratory support, if given during
and young adults 18–24 yrs with
major depressive disorder, other third trimester. Unknown if distributed
psychiatric disorders. Not approved in breast milk. Children: Safety and
for use in children. efficacy not established. Elderly: Severe
Do not confuse Savella with renal impairment requires dosage
cevimeline or sevelamer. adjustment.
uCLASSIFICATION INTERACTIONS
PHARMACOTHERAPEUTIC: Seroto- DRUG: Alcohol, clomipramine,
nin, norepinephrine reuptake inhibi- metoclopramide may increase adverse
tor. CLINICAL: Fibromyalgia agent. effects. May increase adverse effects
of digoxin. Linezolid, MAOIs (e.g.
phenelzine, selegiline) may increase
USES serotonergic effect. EPINEPHrine,
Management of fibromyalgia. norepinephrine may produce parox-
ysmal hypertension, arrhythmias. May
PRECAUTIONS inhibit antihypertensive effect of cloNI-
Contraindications:Hypersensitivity to Dine. HERBAL: Glucosamine, herb-
milnacipran. Concomitant use of MAOIs als with anticoagulant/antiplatelet
to treat psychiatric disorders (concur- activity (e.g., garlic, ginger, ginkgo
rently or within 5 days of discontinuing biloba) may increase adverse effects.
milnacipran or within 2 wks of discon- FOOD: None known. LAB VALUES: May
tinuing MAOI), initiation of milnacipran decrease serum sodium.
underlined – top prescribed drug
milrinone 781

AVAILABILITY (Rx) syndrome symptoms may include men-


tal status changes (agitation, hallucina-
Tablets, Film-Coated: 12.5 mg, 25 tions), hyperreflexia, incoordination. May
mg, 50 mg, 100 mg. increase risk of bleeding events (e.g.,
ecchymoses, hematomas, epistaxis).
ADMINISTRATION/HANDLING
• Give without regard to food. • Do NURSING CONSIDERATIONS
not break, crush, dissolve, or divide film-
coated tablets. BASELINE ASSESSMENT
Obtain baseline pain intensity scale,
INDICATIONS/ROUTES/DOSAGE location(s) of pain, tenderness. Obtain
Fibromyalgia baseline B/P, heart rate. Question for his-
PO: ADULTS, ELDERLY: Day 1: 12.5 mg tory of changes in day-to-day pain intensity.
once. Days 2–3: 25 mg/day (12.5 mg INTERVENTION/EVALUATION
twice daily). Days 4–7: 50 mg/day (25
mg twice daily). After Day 7: 100 mg/day Control nausea with antiemetics. Treat
(50 mg twice daily thereafter). Dose may complaint of headache, migraine with ap-
be increased to 200 mg/day (100 mg twice propriate analgesics. Monitor for increase
daily). in B/P, pulse. Question for changes in
visual acuity. Assess for clinical improve-
Dosage in Renal Impairment ment and record onset of pain control,
Mild impairment: No dose ­adjustment. decreased fatigue, lessening of depressive
symptoms, improvement in sleep pattern. M
Moderate impairment: Use caution.
Severe impairment: Reduce mainte- Monitor for suicidal ideation.
nance dose by 50% to 50 mg/day (25 mg PATIENT/FAMILY TEACHING
twice daily). Based on pt response, dose
may be increased to 100 mg/day (50 mg • Avoid tasks that require alertness, mo-
twice daily). Not recommended in end- tor skills until response to drug is estab-
stage renal disease. lished. • Do not abruptly discontinue
medication. • Increase fluids, bulk to
Dosage in Hepatic Impairment prevent constipation. • Report unusual
Mild to moderate impairment: No changes in behavior, suicidal ideation;
dose adjustment. Severe impairment: hot flushing that becomes intolerant, ex-
Use caution. cessive sweating. • Caution about risk
of bleeding associated with concomitant
SIDE EFFECTS use of NSAIDs, aspirin.
Frequent (37%–18%): Nausea, headache.
Occasional (16%–5%): Constipation, inso­
mnia, hot flashes, dizziness, hyperhi-
drosis, palpitations, vomiting, URI. Rare
milrinone
(less than 5%): Dry mouth, increased
mil-ri-none
B/P, anxiety, skin flushing, rash, blurred
vision, abdominal pain, chest pain, chills, uCLASSIFICATION
pruritus, paresthesia, tachycardia.
PHARMACOTHERAPEUTIC: Cardiac
ADVERSE EFFECTS/TOXIC inotropic agent. CLINICAL: Vasodi-
REACTIONS lator.
Abrupt discontinuation may present with-
drawal symptoms (dysphoria, irritability, USES
agitation, dizziness, paresthesia, anxiety, Short-term management of decompen-
confusion, headache, lethargy, emotional sated HF. OFF-LABEL: Inotropic therapy
lability, tinnitus, seizures). Serotonin
Canadian trade name Non-Crushable Drug High Alert drug
782 milrinone
for pts unresponsive to other therapy, ADMINISTRATION/HANDLING
outpatient inotropic therapy for heart
IV
transplant candidates, palliation of symp-
toms in end-stage HF. Reconstitution • For IV infusion, di-
lute 20-mg (20-mL) vial with 80 mL
PRECAUTIONS 0.9% NaCl or D5W to provide concentra-
Contraindications: Hypersensitivity to tion of 0.2 mg/mL (200 mcg/mL).
milrinone. Cautions: Severe obstruc- Rate of administration • For IV in-
tive aortic or pulmonic valvular dis- jection (loading dose), administer un-
ease, history of ventricular arrhythmias, diluted slowly over 10 min. • Monitor
atrial fibrillation/flutter, renal impair- for arrhythmias, hypotension during IV
ment. Not recommended in pts with therapy; reduce or temporarily discon-
acute MI. tinue infusion until condition stabilizes.
Infuse via infusion pump.
ACTION Storage • Diluted solutions stable for
Inhibits phosphodiesterase, which in 72 hrs at room temperature.
creases cyclic adenosine monophos-
phate (cAMP), potentiating delivery of IV INCOMPATIBILITIES
calcium to myocardial contractile sys- Furosemide (Lasix), imipenem-cilastatin
tems. Therapeutic Effect: Relaxes (Primaxin), procainamide (Pronestyl).
vascular muscle, causing vasodilation.
M Increases cardiac output, decreases IV COMPATIBILITIES
pulmonary capillary wedge pressure, Calcium gluconate, dexamethasone
vascular resistance. (Dec­­adron), dexmedetomidine (Pre-
cedex), digoxin (Lanoxin), dilTIAZem
PHARMACOKINETICS (Cardizem), DOBUTamine (Dobutrex),
Route Onset Peak Duration DOPamine (Intropin), heparin, HYDRO-
IV 5–15 min N/A N/A morphone (Dilaudid), lidocaine, magne-
sium, midazolam (Versed), morphine,
Protein binding: 70%. Metabolized in liver. nitroglycerin, potassium, propofol
Primarily excreted in urine. Half-life: (Diprivan).
1.7–2.7 hrs.
INDICATIONS/ROUTES/DOSAGE
LIFESPAN CONSIDERATIONS Management of HF
Pregnancy/Lactation: Unknown if drug IV: ADULTS: Initially,
50 mcg/kg over
crosses placenta or is distributed in 10 min. Continue with maintenance
breast milk. Children: Safety and effi- infusion rate of 0.125–0.75 mcg/kg/
cacy not established. Elderly: Age-related min based on hemodynamic and clini-
renal impairment may require dosage cal response.
adjustment.
Dosage in Renal Impairment
INTERACTIONS Creatinine Clearance Dosage
DRUG: None significant. HERBAL: None 50 mL/min 0.43 mcg/kg/min
significant. FOOD: None known. LAB 40 mL/min 0.38 mcg/kg/min
VALUES: None significant. 30 mL/min 0.33 mcg/kg/min
20 mL/min 0.28 mcg/kg/min
AVAILABILITY (Rx) 10 mL/min 0.23 mcg/kg/min
5 mL/min 0.2 mcg/kg/min
Injection Solution: (Primacor): 1 mg/
mL, 10-mL vial. Injection Solution, Pre-
mix: (Primacor): 200 mcg/mL (100 mL, Dosage in Hepatic Impairment
200 mL). No dose adjustment.

underlined – top prescribed drug


minocycline 783

SIDE EFFECTS cholerae, Brucella spp.; gram-negative


Occasional (3%–1%): Headache, hypoten- organisms, including acute intestinal ame-
sion. Rare (less than 1%): Angina, chest biasis, gram-negative respiratory and skin/
pain. skin structure infections. Solodyn: Treat-
ment of inflammatory lesions of moderate
ADVERSE EFFECTS/TOXIC to severe nonnodular acne. OFF-LABEL:
REACTIONS Treatment of nocardiosis, community-
Supraventricular/ventricular arrhyth- acquired MRSA infection, rheumatoid
mias (12%), nonsustained ventricular arthritis (RA), prosthetic joint infection.
tachycardia (2%), sustained ventricu-
PRECAUTIONS
lar tachycardia (1%) may occur. Ven-
tricular fibrillation (0.2%) has been Contraindications: Hypersensitivity to
documented. minocycline, other tetracyclines. Cau-
tions: Children younger than 8 yrs, renal
NURSING CONSIDERATIONS impairment, hepatic impairment, sun/
ultraviolet exposure (severe photosensi-
BASELINE ASSESSMENT tivity reaction). Avoid use in pregnancy.
Obtain baseline lab studies, esp. BN pep-
tide. Offer emotional support (difficulty ACTION
breathing may produce anxiety). Assess Inhibits bacterial protein synthesis by
B/P, apical pulse rate before treatment binding to ribosomes. Therapeutic
begins and during IV therapy. Assess lung Effect: Bacteriostatic. M
sounds; observe for edema.
PHARMACOKINETICS
INTERVENTION/EVALUATION
Well absorbed from GI tract. Protein bind-
Monitor B/P, heart rate, cardiac output, ing: 70%–75%. Partially excreted in feces;
ECG, serum potassium, renal function, minimal excretion in urine. Not removed
signs/symptoms of HF. by hemodialysis. Half-life: 11–23 hrs.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Readily crosses
minocycline placenta; distributed in breast milk. May
inhibit fetal skeletal growth. Children: May
mye-noe-sye-kleen cause permanent discoloration of teeth,
(CoreMino, Monolira, Ximino, enamel hypoplasia. Not recommended in
Minocin, Solodyn) pts younger than 8 yrs. Elderly: No age-
Do not confuse Dynacin with related precautions noted.
Dyazide, DynaCirc, or Dynapen,
or Minocin with Indocin, Mith- INTERACTIONS
racin, or niacin. DRUG: Bile acid sequestrants (e.g.,
cholestyramine) may decrease
uCLASSIFICATION absorption. Aluminum-, calcium-,
PHARMACOTHERAPEUTIC: Tetracy- magnesium-containing antacids
cline. CLINICAL: Antibiotic. may decrease absorption, effect. May
decrease the effects of estrogen-con-
taining oral contraceptives. HERBAL:
USES St. John’s wort may decrease concen-
Treatment of susceptible infections due to tration/effect. FOOD: None known. LAB
Rickettsiae, M. pneumoniae, C. tracho- VALUES: May increase serum alkaline
matis, C. psittaci, H. ducreyi, Yersinia phosphatase, amylase, bilirubin, ALT,
pestis, Francisella tularensis, Vibrio AST, BUN.

Canadian trade name Non-Crushable Drug High Alert drug


784 mirabegron

AVAILABILITY (Rx) ADVERSE EFFECTS/TOXIC


Capsules: 50 mg, 75 mg, 100 mg. Tab- REACTIONS
lets: 50 mg, 75 mg, 100 mg. Superinfection (esp. fungal), anaphy-
Capsules, Extended-Release: 90 mg, laxis, increased ICP may occur. Bulging
135 mg. Tablets, Extended-Release: 45 fontanelles occur rarely in infants.
mg, 55 mg, 65 mg, 80 mg, 90 mg, 105
mg, 115 mg, 135 mg. NURSING CONSIDERATIONS
ADMINISTRATION/HANDLING BASELINE ASSESSMENT

PO Question for history of allergies, esp. tet-


• Take without regard to food. • Give racyclines, sulfite.
with adequate fluid (reduces risk of INTERVENTION/EVALUATION
esophageal irritation and ulceration). Assess ability to ambulate (may cause ver-
• Give pellet-filled capsules, extended- tigo, dizziness). Monitor daily pattern of
release tablets whole; do not cut, crush, bowel activity, stool consistency. Monitor
dissolve, or divide. renal function, LFT with long-term therapy.
INDICATIONS/ROUTES/DOSAGE Assess skin for rash. Observe for signs of
Usual Dosage increased intracranial pressure (altered
PO: ADULTS, ELDERLY: Initially, 100–200 LOC, widened pulse pressure). Be alert
mg once, then 100 mg q12h or 50 mg 4 for superinfection: fever, vomiting, diar-
M times/day. CHILDREN OLDER THAN 8 YRS: Ini- rhea, anal/genital pruritus, oral mucosal
tially, 4 mg/kg once, then 2 mg/kg q12h. changes (ulceration, pain, erythema).
Maximum: 100 mg/dose, 200 mg/day. PATIENT/FAMILY TEACHING
Acne • Continue antibiotic for full length of
PO: (CoreMino, Solodyn): CHILDREN treatment. • Space doses evenly. • Drink
12 YRS AND OLDER, WEIGHING 126–136 full glass of water with capsules or tab-
KG: 135 mg once daily; 111–125 KG: 115 lets. • Avoid tasks that require alertness,
mg once daily; 97–110 KG: 105 mg once motor skills until response to drug is estab-
daily; 85–96 KG: 90 mg once daily; 72–84 lished. • Report diarrhea, rash, other
KG: 80 mg once daily; 60–71 KG: 65 mg new symptoms. • Protect skin from sun
once daily; 50–59 KG: 55 mg once daily; exposure. • Advise female pts to use ad-
45–49 KG: 45 mg once daily. (Ximino): ditional form of birth control (may de-
1 mg/kg (round to nearest size) once crease effectiveness of oral contraceptives).
daily. (Minolira) 12–136 KG: 135 mg once
daily. 90–125 KG: 105 mg once daily. 60–­
89 KG: 67.5 mg once daily. 45–59 KG: 52.5 mirabegron
mg once daily. (Capsule or Imme-
diate-Release Tablet): ADULTS, mir-a-beg-ron
ELDERLY: 50–100 mg/twice daily. (Myrbetriq)
Dosage in Renal/Hepatic Impairment uCLASSIFICATION
Use caution.
PHARMACOTHERAPEUTIC: Beta 3 -
SIDE EFFECTS adrenergic agonist. CLINICAL: Smooth
Frequent: Dizziness, light-headedness, diar- muscle relaxant.
rhea, nausea, vomiting, abdominal cramps,
possibly severe photosensitivity, drowsiness, USES
vertigo. Occasional: Altered pigmentation Treatment of overactive bladder with symp-
of skin, mucous membranes, rectal/genital toms of urinary incontinence, urgency, fre-
pruritus, stomatitis. quency as monotherapy or in combination
with solifenacin.
underlined – top prescribed drug
mirabegron 785

PRECAUTIONS ADMINISTRATION/HANDLING
Contraindications: Hypersensitivity to mira- PO
begron. Cautions: Bladder outlet obstruc- • Give without regard to food. • Ad-
tion, pts taking antimuscarinic medications minister with water; instruct pt to swal-
(increases urinary retention), mild to low whole. • Do not break, crush,
moderate hepatic/renal impairment, his- dissolve, or divide film-coated tablets.
tory of QT-interval prolongation, medica-
tions known to prolong QT interval. Not INDICATIONS/ROUTES/DOSAGE
recommended for use in pts with severe Overactive Bladder
uncontrolled hypertension (SBP equal to or PO: ADULTS, ELDERLY: (Monotherapy):
greater than 180 mm Hg and/or DBP equal Initially, 25 mg once daily. Efficacy
to or greater than 110 mm Hg). seen within 8 wks for 25-mg dose. May
increase to 50 mg once daily. (Combi-
ACTION nation with solifenacin): Initially, 25
Relaxes detrusor smooth muscle of blad- mg once daily with solifenacin 5 mg once
der through beta3 stimulation during daily. May increase mirabegron to 50 mg
storage phase of urinary bladder fill–void once daily after 4–8 wks.
cycle. Therapeutic Effect: Increases
bladder capacity, reduces symptoms of Dosage in Renal Impairment
urinary urgency, increased voiding fre- Mild to moderate impairment: No
quency, urge incontinence, nocturia. dosage adjustment. Severe impair-
ment: Do not exceed 25 mg once daily. M
PHARMACOKINETICS
Dosage in Hepatic Impairment
Readily absorbed following PO adminis-
Mild impairment: No dosage adjust-
tration; widely distributed. Protein bind-
ing: 71%. Eliminated in urine (55%), ment. Moderate impairment: Do not
feces (35%). Half-life: 50 hrs. exceed 25 mg once daily. Severe impair-
ment: Not recommended.
LIFESPAN CONSIDERATIONS
SIDE EFFECTS
Pregnancy/Lactation: Unknown if dis-
tributed in breast milk. Children: Safety Occasional (9%–4%): Hypertension, head-
and efficacy not established. Elderly: No ache, nasopharyngitis. Rare (2%–1%): Con-
age-related precautions noted. stipation, arthralgia, diarrhea, tachycardia,
fatigue.
INTERACTIONS
ADVERSE EFFECTS/TOXIC
DRUG: May increase concentration/ REACTIONS
effects of desipramine, digoxin, thio-
ridazine, flecainide, propafenone. Worsening of preexisting hypertension
May decrease concentration/effect of reported infrequently. Urinary tract infec-
tamoxifen. HERBAL: None signifi- tion occurred in 6% of pts, influenza in
cant. FOOD: None known. LAB VALUES: 3%, and upper respiratory infection in
May increase GGT, LDH; temporarily 1.5%.
increase ALT, AST. NURSING CONSIDERATIONS
AVAILABILITY (Rx) BASELINE ASSESSMENT
Tablets, Extended-Release: 25 mg, Check B/P; assess for hypertension. Mon-
50 mg. itor ECG. Receive full medication history,
and screen for possible drug interac-
tions. Monitor I&O (particularly in pts
with history of urinary retention).

Canadian trade name Non-Crushable Drug High Alert drug


786 mirtazapine

INTERVENTION/EVALUATION PRECAUTIONS
Monitor ALT, AST, LDH, GGT periodi- Contraindications: Hypersensitivity to mir-
cally. Palpate bladder for urinary reten- tazapine. Use of MAOIs to treat psychiat-
tion. Measure B/P near end of dosing ric disorders (concurrently or within 14
interval (determines whether B/P is days of discontinuing either MAOI or mir-
controlled throughout day). Periodic tazapine), initiation of mirtazapine in pts
B/P determinations are recommended, receiving linezolid or IV methylene blue.
especially in hypertensive pts. For pts Cautions: Renal/hepatic impairment,
taking digoxin, monitor digoxin serum elderly pts, seizure disorder, suicidal
level for therapeutic effect (very nar- ideation or behavior, alcoholism, con-
row line between therapeutic and toxic current medications that lower seizure
level). Assess pulse for quality, irregular threshold, cardiovascular disease, pts at
rate, bradycardia. Question for evidence risk for QT prolongation, medications
of headache. known to prolong QT interval.
PATIENT/FAMILY TEACHING ACTION
• Report urinary retention. • Do not Acts as antagonist at presynaptic alpha2-
use nasal decongestants, over-the-counter adrenergic receptors, increasing norepi-
cold preparations without doctor ap- nephrine, serotonin neurotransmission.
proval. Restrict salt, alcohol intake. Has low anticholinergic activity. Thera-
• Take mirabegron with water; swallow peutic Effect: Relieves depression.
M tablet whole; do not chew, crush, dis-
solve, or divide tablet. • May take with PHARMACOKINETICS
or without food. Rapidly, completely absorbed after PO
administration; absorption not affected
by food. Protein binding: 85%. Metabo-
lized in liver. Primarily excreted in urine.
Unknown if removed by hemodialysis.
mirtazapine Half-life: 20–40 hrs (longer in males
[37 hrs] than females [26 hrs]).
mir-taz-a-peen
(Remeron, Remeron Soltab) LIFESPAN CONSIDERATIONS
j BLACK BOX ALERT jIncreased Pregnancy/Lactation: Unknown if dis-
risk of suicidal thinking and behav- tributed in breast milk. Children: Safety
ior in children, adolescents, young and efficacy not established. Elderly: Age-
adults 18–24 yrs with major depres- related renal impairment may require dos-
sive disorder, other psychiatric
disorders. age adjustment.
Do not confuse Remeron INTERACTIONS
with Premarin, Rozerem, or
Zemuron. DRUG: Alcohol, CNS depressant
medications (e.g., LORazepam,
uCLASSIFICATION morphine, zolpidem) may increase
PHARMACOTHERAPEUTIC: Alpha-2 impairment of cognition, motor skills.
antagonist. CLINICAL: Antidepres- Serotonergic drugs (e.g., venla-
sant. faxine) may increase risk of serotonin
syndrome. Strong CYP3A4 inducers
(e.g., carBAMazepine, phenytoin,
USES rifAMPin) may decrease concentration/
Treatment of major depressive disorder effects. Strong CYP3A4 inhibitors
(MDD). (e.g., clarithromycin, ketoconazole,
ritonavir) may increase concentration/
underlined – top prescribed drug
miSOPROStol 787
effects. MAOIs (e.g., phenelzine, sele- ADVERSE EFFECTS/TOXIC
giline) may increase risk of neuroleptic REACTIONS
malignant syndrome, hypertensive crisis, Higher incidence of seizures than with
severe seizures. HERBAL: Herbals with tricyclic antidepressants (esp. in pts with
sedative properties (e.g., chamomile, no history of seizures). Overdose may
kava kava, valerian) may increase CNS produce cardiovascular effects (severe
depression. St. John’s wort may decrease orthostatic hypotension, dizziness, tachy-
concentration/effects, may increase risk of cardia, palpitations, arrhythmias). Abrupt
serotonin syndrome. FOOD: None known. discontinuation from prolonged therapy
LAB VALUES: May increase serum choles- may produce headache, malaise, nausea,
terol, triglycerides, ALT. vomiting, vivid dreams. Agranulocytosis
occurs rarely.
AVAILABILITY (Rx)
Tablets: 7.5 mg, 15 mg, 30 mg, 45 mg. NURSING CONSIDERATIONS
Tablets, Orally Disintegrating: 15 mg, 30
mg, 45 mg. BASELINE ASSESSMENT
Assess mental status, appearance, be-
ADMINISTRATION/HANDLING havior, speech pattern, level of interest,
PO mood. Obtain baseline weight. For pts on
• Give without regard to food. • May long-term therapy, renal function, LFT,
crush/break scored tablets. CBC should be performed periodically.
INTERVENTION/EVALUATION
M
Orally Disintegrating Tablets
• Give without regard to food. • Do Supervise suicidal-risk pt closely during
not split tablet. • Place on tongue; dis- early therapy (as depression lessens, en-
solves without water. ergy level improves, increasing suicide
potential). Children, adolescents are at
INDICATIONS/ROUTES/DOSAGE increased risk for suicidal thoughts/be-
Depression havior and worsening of depression, esp.
Note: When discontinuing, gradually during first few mos of therapy. Assess ap-
taper dose to minimize withdrawal symp- pearance, behavior, speech pattern, level
toms and to allow detection of re-emerg- of interest, mood. Monitor for hypoten-
ing symptoms. PO: ADULTS: Initially, 15 sion, arrhythmias.
mg at bedtime. May increase by 15 mg/ PATIENT/FAMILY TEACHING
day q1–2wks. Maximum: 45 mg/day.
ELDERLY: Initially, 7.5 mg at bedtime. May
• Take as single bedtime dose. • Avoid
increase by 7.5–15 mg/day q1–2wks. alcohol, depressant/sedating medica-
Maximum: 45 mg/day. tions. • Avoid tasks requiring alertness,
motor skills until response to drug estab-
Dosage in Renal/Hepatic Impairment lished. • Report worsening depression,
Use caution. suicidal ideation, unusual changes in
behavior.
SIDE EFFECTS
Frequent (54%–12%): Drowsiness, dry
mouth, increased appetite, constipation,
weight gain. Occasional (89%–4%): Asthe- miSOPROStol
nia, dizziness, flu-like symptoms, abnormal
dreams. Rare: Abdominal discomfort, mis-oh-pros-tol
vasodilation, paresthesia, acne, dry skin, (Cytotec)
thirst, arthralgia. j BLACK BOX ALERT jUse dur-
ing pregnancy can cause abortion,
premature birth, birth defects.

Canadian trade name Non-Crushable Drug High Alert drug


788 miSOPROStol

Not recommended in women of in urine. Unknown if removed by hemo-


childbearing potential unless pt is dialysis. Half-life: 20–40 min.
capable of complying with effective
contraception. LIFESPAN CONSIDERATIONS
Do not confuse Cytotec with Pregnancy/Lactation: Unknown if dis-
Cytoxan, or miSOPROStol with tributed in breast milk. Produces uterine
metoprolol or miFEPRIStone. contractions, uterine bleeding, expulsion
FIXED-COMBINATION(S) of products of conception (abortifacient
property). Children: Safety and efficacy
Arthrotec: miSOPROStol/diclofenac not established. Elderly: No age-related
(an NSAID): 200 mcg/50 mg, 200 precautions noted.
mcg/75 mg.
INTERACTIONS
uCLASSIFICATION
DRUG: Antacids may increase con-
PHARMACOTHERAPEUTIC: Prosta- centration. May increase adverse
glandin. CLINICAL: Antisecretory, gas- effects of oxytocin. HERBAL: None
tric protectant. significant. FOOD: None known. LAB
VALUES: None significant.
USES
AVAILABILITY (Rx)
Prevention of NSAID-induced gastric ulcers
Tablets: 100 mcg, 200 mcg.
M and in pts at high risk for developing gastric
ulcer/gastric ulcer complications. Medi- ADMINISTRATION/HANDLING
cal termination of intrauterine pregnancy
PO
through 70 days’ gestation (in conjunction
• Give with or after meals (minimizes
with miFEPRIStone). OFF-LABEL: Cervical
diarrhea).
ripening, labor induction, treatment/pre-
vention of postpartum hemorrhage, treat- INDICATIONS/ROUTES/DOSAGE
ment of incomplete or missed abortion.
Prevention of NSAID-Induced Gastric
PRECAUTIONS Ulcer
PO: ADULTS, ELDERLY: 200 mcg 4 times/
Contraindications: Hypersensitivity to
day with food (last dose at bedtime). Con-
misoprostol, other prostaglandins; preg-
tinue for duration of NSAID therapy. May
nancy. Cautions: Renal impairment, car-
reduce dosage to 100 mcg 4 times/day.
diovascular disease, elderly.
ACTION Termination of Intrauterine Pregnancy
See manufacturer guidelines for miFE-
Replaces protective prostaglandins PRIstne.
consumed with prostaglandin-inhib-
iting therapies (e.g., NSAIDs). Induces Early Pregnancy Loss
uterine contractions. Therapeutic Intravaginal: 800 mcg once; may repeat
Effect: Reduces acid secretion from 3 or more hrs after first dose and within 7
gastric parietal cells, stimulates bicar- days of no response to initial dose.
bonate production from gastric/duode-
nal mucosa. Incomplete Abortion, Postpartum
Hemorrhage
PHARMACOKINETICS PO: 600 mcg as a single dose.
Route Onset Peak Duration
Labor Induction or Cervical Ripening
PO 30 min 1–1.5 hrs 3–6 hrs
Intravaginal: 25 mcg q3–6 hrs. Some
Rapidly absorbed from GI tract. Protein pts may require 50 mcg q6hrs. Maxi-
binding: 80%–90%. Primarily excreted mum: 50 mcg/dose.
underlined – top prescribed drug
mitoMYcin 789
Postpartum Hemorrhage (Prevention) istered by certified chemotherapy
PO: ADULTS: 600 mcg as a single dose personnel.
given immediately after delivery. Do not confuse mitoMYcin with
mithramycin or mitoXANTRONE.
Postpartum Hemorrhage (Treatment)
PO/Rectal: ADULTS: 600–1,000 mcg as uCLASSIFICATION
a single dose. PHARMACOTHERAPEUTIC: Antibi-
otic. CLINICAL: Antineoplastic.
Dosage in Renal/Hepatic Impairment
No dose adjustment.
USES
SIDE EFFECTS Treatment of disseminated adenocarci-
Frequent (40%–20%): Abdominal pain, noma of stomach, pancreas (in combina-
diarrhea. Occasional (3%–2%): Nausea, tion with other chemotherapy agents and
flatulence, dyspepsia, headache. Rare as palliative treatment when other modal-
(1%): Vomiting, constipation. ities have failed). OFF-LABEL: Treatment
of bladder cancer, anal carcinoma; cervi-
ADVERSE EFFECTS/TOXIC cal, esophageal, gastric, non–small-cell
REACTIONS lung cancer.
Overdosage may produce sedation,
tremor, seizures, dyspnea, palpitations, PRECAUTIONS
hypotension, bradycardia. Contraindications: Hypersensitivity to M
mitomycin. Coagulation disorders, other
NURSING CONSIDERATIONS increased bleeding tendencies, throm-
BASELINE ASSESSMENT bocytopenia. Cautions: Myelosuppres-
Question for possibility of pregnancy be- sion, renal (serum creatinine greater
fore initiating therapy. than 1.7 mg/dL)/hepatic impairment,
pregnancy, prior radiation treatment.
PATIENT/FAMILY TEACHING
• Avoid magnesium-containing antacids ACTION
(minimizes potential for diarrhea). Alkylating agent, produces DNA cross-
• Women of childbearing potential must linking. Therapeutic Effect: Inhibits
not be pregnant before or during medi- DNA, RNA synthesis.
cation therapy (may result in hospitaliza-
tion, surgery, infertility, fetal death). PHARMACOKINETICS
• Incidence of diarrhea may be less- Widely distributed. Does not cross blood-
ened by taking immediately following brain barrier. Metabolized in liver. Excreted
meals. in urine. Half-life: 50 min.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: If possible, avoid
mitoMYcin use during pregnancy, esp. first trimes-
ter. Breastfeeding not recommended.
mye-toe-mye-sin Safety in pregnancy not established. Chil-
(Mutamycin) dren: Safety and efficacy not established.
j BLACK BOX ALERT jPotent Elderly: Age-related renal impairment
vesicant. Marked myelosup- may require dosage adjustment.
pression. Infiltration produces
ulceration, necrosis, cellulitis, INTERACTIONS
tissue sloughing. Hemolytic-uremic
syndrome reported. Must be admin- DRUG: Bone marrow depressants
(e.g., cladribine) may increase

Canadian trade name Non-Crushable Drug High Alert drug


790 mitoMYcin
myelosuppression. Live virus vaccines upogen), heparin, piperacillin/tazobactam
may potentiate virus replication, increase (Zosyn), sargramostim (Leukine), vinorel-
vaccine side effects, decrease pt’s antibody bine (Navelbine).
response to vaccine. HERBAL: Echina-
cea may decrease the therapeutic effect. IV COMPATIBILITIES
FOOD: None known. LAB VALUES: May Cisplatin (Platinol AQ), cyclophospha-
increase serum BUN, creatinine. mide (Cytoxan), DOXOrubicin (Adriamy-
cin), 5-fluorouracil, granisetron (Kytril),
AVAILABILITY (Rx) leucovorin, methotrexate, ondansetron
Injection, Powder for Reconstitution: 5 (Zofran), vinBLAStine (Velban), vinCRIS-
mg, 20 mg, 40 mg. tine (Oncovin).
ADMINISTRATION/HANDLING INDICATIONS/ROUTES/DOSAGE
b ALERT c May be carcinogenic, muta- Stomach, Pancreatic Cancer
genic, teratogenic. Handle with extreme IV: ADULTS, ELDERLY, CHILDREN: 20 mg/
care during preparation/administration. m2 as single dose. Repeat q6–8wks.
Give via IV push, IV infusion. Extremely
irritating to vein. Injection may produce Bladder Cancer (Non–Muscle Invasive)
pain with induration, thrombophlebitis, Intravesicular Instillation: ADULTS,
paresthesia. ELDERLY: Low risk of recurrence: 40 mg
as single dose postoperatively (retain in
M IV
bladder for 1–2 hrs). High risk of recur-
Reconstitution • Reconstitute with rence: 20 mg/wk for 6 wks, then 20 mg
Sterile Water for Injection to provide solu- qmo for 3 yrs (retain in bladder for 1–2
tion containing 0.5–1 mg/mL. • Do not hrs).
shake vial to dissolve. • Allow vial to
stand at room temperature until complete Dose Modification for Toxicity
dissolution occurs. • For IV infusion, fur- Leukocytes 2,000 to Hold therapy until
ther dilute with 50–100 mL D5W or 0.9% less than 3,000 leukocytes 4,000 or
NaCl (concentration 20–40 mcg/mL). cells/mm3 more cells/mm3; re-
Rate of administration • Give slow duce dose to 70%
IV push or by IV infusion over 15–30 or more in subse-
quent cycles
min. • Extravasation may produce cel-
lulitis, ulceration, tissue sloughing. Ter- Leukocytes less Hold therapy until
than 2,000 cells/ leukocytes 4,000
minate administration immediately,
mm3 or more cells/mm3;
inject ordered antidote. Apply ice inter- reduce dose to
mittently for up to 72 hrs; keep area 50% in subse-
elevated. quent cycles
Storage • Use only clear, blue-gray Platelets 25,000 to Hold therapy until
solutions. • Concentration of 0.5 mg/ less than 75,000 platelets 100,000
mL (reconstituted vial or syringe) is sta- cells/mm3 or more cells/mm3;
ble for 7 days at room temperature or 2 reduce dose to
70% in subse-
wks if refrigerated. Further diluted solu-
quent cycles
tion with D5W is stable for 3 hrs, 12 hrs Platelets less than Hold therapy until
if diluted with 0.9% NaCl at room tem- 25,000 cells/mm 3 platelets 100,000
perature. or more cells/mm3;
reduce dose to
IV INCOMPATIBILITIES 50% in subse-
Aztreonam (Azactam), bleomycin (Blenox- quent cycles
ane), cefepime (Maxipime), filgrastim (Ne-

underlined – top prescribed drug


modafinil 791

Dosage in Renal Impairment PATIENT/FAMILY TEACHING


CrCl less than 10 mL/min: Give 75% • Maintain strict oral hygiene. • Imme-
of normal dose. diately report stinging, burning, pain at in-
Dosage in Hepatic Impairment
jection site. • Do not have immunizations
No dose adjustment. without physician’s approval (drug lowers
resistance to infection). • Avoid contact
SIDE EFFECTS with those who have recently received live
Frequent (greater than 10%): Fever,
virus vaccine. • Hair loss is reversible,
anorexia, nausea, vomiting. Occasional but new hair growth may have different
(10%–2%): Stomatitis, paresthesia, purple
color, texture. • Report nausea/vomiting,
colored bands on nails, rash, alope- fever, sore throat, bruising, bleeding, short-
cia, unusual fatigue. Rare (less than ness of breath, painful urination.
1%): Thrombophlebitis, cellulitis with
extravasation.
ADVERSE EFFECTS/TOXIC modafinil
REACTIONS
Marked myelosuppression results in moe-daf-i-nil
hematologic toxicity manifested as leuko- (Alertec , Provigil)
penia, thrombocytopenia, and, to a lesser uCLASSIFICATION
extent, anemia (generally occurs within M
2–4 wks after initial therapy). Renal PHARMACOTHERAPEUTIC: Alpha1-
toxicity may be evidenced by increased agonist, CNS stimulant (Schedule IV).
CLINICAL: Wakefulness-promoting
serum BUN, creatinine levels. Pulmonary
toxicity manifested as dyspnea, cough, agent, antinarcoleptic.
hemoptysis, pneumonia. Long-term
therapy may produce hemolytic uremic USES
syndrome, characterized by hemolytic
Treatment of excessive daytime sleepiness
anemia, thrombocytopenia, renal failure,
associated with narcolepsy, shift work sleep
hypertension.
disorder, adjunct therapy for obstructive
NURSING CONSIDERATIONS sleep apnea/hypopnea syndrome. OFF-
LABEL: Treatment of ADHD, multiple scle-
BASELINE ASSESSMENT rosis–related fatigue.
Obtain CBC with differential, PT, bleed-
ing time, before and periodically during PRECAUTIONS
therapy. Antiemetics before and during Contraindications: Hypersensitivity to moda­
therapy may alleviate nausea/vomit- finil, armodafinil. Cautions: History of
ing. Offer emotional support. clinically significant mitral valve prolapse, left
ventricular hypertrophy, renal/hepatic impair-
INTERVENTION/EVALUATION ment, angina, cardiac disease, myocardial
Monitor hematologic status, renal func- ischemia, recent MI, preexisting psychosis or
tion studies. Assess IV site for phlebitis, bipolar disorder, Tourette’s syndrome.
extravasation. Monitor for hematologic
toxicity (fever, sore throat, signs of lo- ACTION
cal infection, unusual bruising/bleed- Exact mechanism unknown. Increases
ing from any site), symptoms of anemia dopamine in brain. Increases alpha activ-
(excessive fatigue, weakness). Assess for ity, decreasing delta, theta, brain wave
renal toxicity (foul odor from urine, el- activity. Therapeutic Effect: Reduces
evated serum BUN, creatinine). number of sleep episodes, total daytime
sleep. Increases mental alertness.
Canadian trade name Non-Crushable Drug High Alert drug
792 mometasone
PHARMACOKINETICS SIDE EFFECTS
Well absorbed from GI tract. Pro- Generally well tolerated. Occasional
tein binding: 60%. Widely distributed. (5%): Headache, nausea, dizziness, insom-
Metabolized in liver. Excreted by kidneys. nia, palpitations, diarrhea.
Unknown if removed by hemodialysis.
Half-life: 15 hrs. ADVERSE EFFECTS/TOXIC
REACTIONS
LIFESPAN CONSIDERATIONS Agitation, excitation, increased B/P, insom-
Pregnancy/Lactation: Unknown if ex- nia may occur. Psychiatric disturbances
creted in breast milk. Use caution if given (anxiety, hallucinations, suicidal ideation),
to pregnant women. Children: Safety serious allergic reactions (angioedema, Ste-
and efficacy not established in pts young- vens-Johnson syndrome) have been noted.
er than 16 yrs. Elderly: Age-related
renal/hepatic impairment may require NURSING CONSIDERATIONS
decreased dosage. BASELINE ASSESSMENT
INTERACTIONS Obtain baseline evidence of narcolepsy
DRUG: May decrease concentration/effect or other sleep disorders, including pat-
of cycloSPORINE, oral contraceptives. tern, environmental situations, length of
Alcohol may decrease therapeutic effect. sleep episodes. Question for sudden loss
Strong CYP3A4 inducers (e.g., carBA- of muscle tone (cataplexy) precipitated
M Mazepine, phenytoin, rifAMPin) may by strong emotional responses before
decrease concentration/effect. HERBAL: St. sleep episode. Assess frequency/severity
John’s wort may decrease concentra- of sleep episodes before drug therapy.
tion/effect. FOOD: None known. LAB VAL- INTERVENTION/EVALUATION
UES: None significant. Monitor sleep pattern, evidence of rest-
AVAILABILITY (Rx) lessness during sleep, length of insomnia
episodes at night. Assess for dizziness,
Tablets: (Provigil): 100 mg, 200 mg. anxiety; initiate fall precautions.
ADMINISTRATION/HANDLING PATIENT/FAMILY TEACHING
PO • Avoid alcohol. • Sugarless gum, sips
• Give without regard to food. of water may relieve dry mouth. • Do
not increase dose without physician ap-
INDICATIONS/ROUTES/DOSAGE proval. • Use alternative contraceptives
Narcolepsy, Obstructive Sleep Apnea/ during therapy and 1 mo after discon-
Hypopnea Syndrome tinuing modafinil (reduces effectiveness
PO: ADULTS: 200 mg/day in the morning. of oral contraceptives).
ELDERLY: 100 mg/day in the morning.
Shift Work Sleep Disorder
PO: ADULTS: 200 mg about 1 hr before mometasone
start of work shift.
moe-met-a-sone
Dosage in Renal Impairment (Asmanex, Asmanex HFA, Elocon,
No dose adjustment. Nasonex, Apo-Mometasone )
Dosage in Hepatic Impairment FIXED-COMBINATION(S)
Mild to moderate impairment: No Dulera: mometasone/formoterol
dose adjustment. Reduce dose 50% with (beta-adrenergic agonist): 100 mcg/5
severe impairment. mcg, 200 mcg/5 mcg.

underlined – top prescribed drug


mometasone 793

uCLASSIFICATION cortisol secretion. Elderly: No age-related


precautions noted.
PHARMACOTHERAPEUTIC: Adreno-
corticosteroid. CLINICAL: Anti-infla­ INTERACTIONS
mmatory. DRUG: May increase hyponatremic
effect of desmopressin. May increase
USES antineoplastic effect of aldesleukin.
HERBAL: None significant. FOOD: None
Nasal: Treatment of nasal symptoms of known. LAB VALUES: None significant.
seasonal/perennial allergic rhinitis in
adults, children 2 yrs and older. Relief of AVAILABILITY (Rx)
nasal symptoms of seasonal allergic rhi- Cream: (Elocon): 0.1%. Lotion: (Elocon):
nitis in adults, children 2 yrs and older. 0.1%. Nasal Spray: (Nasonex): 50 mcg/
Treatment of nasal polyps in adults. spray. Ointment: (Elocon): 0.1%. Powder for
Inhalation: Maintenance treatment of Oral Inhaler: (Asmanex): 110 mcg (delivers
asthma as prophylactic therapy in adults 100 mcg/actuation), 220 mcg (delivers 200
and children 4 yrs and older. Topical: mcg/actuation). (Asmanex HFA): 100 mcg/
Relief of inflammatory, pruritic manifes- actuation, 200 mcg/actuation.
tations of steroid-responsive dermatoses.
ADMINISTRATION/HANDLING
PRECAUTIONS
Inhalation
Contraindications: Hypersensitivity to • Do not shake or prime. • Hold twist- M
mometasone, milk proteins. Asmanex: haler straight up with pink portion
Primary treatment of status asthmaticus or (base) on bottom, remove cap. • Ex-
acute bronchospasm. Cautions: Thyroid/ hale fully. • Firmly close lips around
hepatic/renal impairment, elderly, dia- mouthpiece and inhale a fast, deep
betes, cardiovascular disease, glaucoma, breath. • Hold breath for 10 sec.
cataracts, myasthenia gravis, pts at risk for
osteoporosis, seizures, GI disease (e.g., Intranasal
ulcer, colitis); following MI. Untreated sys- • Instruct pt to clear nasal passages as
temic fungal, viral, bacterial infections. much as possible before use. • Tilt
head slightly forward. • Insert spray tip
ACTION into nostril, pointing toward nasal pas-
Inhibits formation, release, and activity sages, away from nasal septum. • Spray
of mediators of inflammation (e.g., hista- into one nostril while pt holds other
mine, kinins). Reverses the dilation and nostril closed, concurrently inspires
increased nasal permeability of inflam- through nose to permit medication as
mation. Therapeutic Effect: Improves high into nasal passages as possible.
symptoms of asthma, rhinitis.
Topical
PHARMACOKINETICS • Apply thin layer of cream, lotion, oint-
Undetectable in plasma. Protein binding: ment to cover affected area. Rub in gen-
98%–99%. Swallowed portion undergoes tly. • Do not cover area with occlusive
extensive metabolism. Excreted in bile dressing.
(74%), urine (8%). Half-life: 5 hrs.
INDICATIONS/ROUTES/DOSAGE
LIFESPAN CONSIDERATIONS Allergic Rhinitis
Pregnancy/Lactation: Unknown if drug Nasal Spray: ADULTS, ELDERLY, CHIL-
crosses placenta or is distributed in breast DREN 12 YRS AND OLDER: 2 sprays (100
milk. Children: Prolonged treatment/high mcg) in each nostril once daily. Total daily
doses may decrease short-term growth rate, dose: 200 mcg. When used to prevent

Canadian trade name Non-Crushable Drug High Alert drug


794 montelukast
nasal rhinitis, begin 2–4 wks before start
of pollen season. CHILDREN 2–11 YRS: 1 NURSING CONSIDERATIONS
spray (50 mcg) in each nostril once daily. BASELINE ASSESSMENT
Total daily dose: 100 mcg. Question for hypersensitivity to any cor-
Asthma ticosteroids.
Inhalation: ADULTS, ELDERLY, CHILDREN INTERVENTION/EVALUATION
12 YRS AND OLDER (Previous therapy with
Teach proper use of nasal spray, oral in-
bronchodilators): (Asmanex): Initially,
haler. Instruct pt to clear nasal passages
inhale 220 mcg (1 puff) once daily. Maxi- before use. Report if no improvement in
mum: 440 mcg/day as single or 2 divided symptoms or if sneezing, nasal irritation
doses. (Previous therapy with inhaled corti- occur. Assess lung sounds for wheezing,
costeroids): (Asmanex HFA): Initially,
rales.
200 mcg twice daily. Maximum: 400
mcg twice daily. (Previous therapy with oral PATIENT/FAMILY TEACHING
corticosteroids): (Asmanex): 440 mcg (2 • Do not change dose schedule or stop
puffs) twice daily. (Asmanex HFA): 400 taking drug; must taper off gradually un-
mcg twice daily. Reduce predniSONE no der medical supervision. Nasal: Report
faster than 2.5 mg/day beginning after at if symptoms do not improve; report if
least 1 wk of mometasone. CHILDREN 4–11 sneezing, nasal irritation occur. • Clear
YRS: (Asmanex): 110 mcg once daily in nasal passages prior to use. Inhalation:
M evening. Inhale rapidly, deeply; rinse mouth after
inhalation. • Not indicated for acute
Skin Disease
asthma attacks. Topical: Do not cover
Topical: ADULTS, ELDERLY, CHILDREN 12 YRS
affected area with bandage, dressing.
AND OLDER: Apply cream, lotion, or oint-
ment sparingly to affected area once daily.
Nasal Polyp
Nasal Spray: ADULTS, ELDERLY: 2 sprays montelukast
(100 mcg) in each nostril once or twice
daily. Total daily dose: 400 mcg. mon-tee-loo-kast
(Singulair)
Dosage in Renal/Hepatic Impairment Do not confuse Singulair with
No dose adjustment. SINEquan.

SIDE EFFECTS uCLASSIFICATION


Occasional: Inhalation: Headache, aller- PHARMACOTHERAPEUTIC: Leukot-
gic rhinitis, upper respiratory infection, riene receptor inhibitor. CLINICAL:
muscle pain, fatigue. Nasal: Nasal irritation, Antiasthmatic.
stinging. Topical: Burning. Rare: Inhala-
tion: Abdominal pain, dyspepsia, nausea.
Nasal: Nasal/pharyngeal candidiasis. Topi- USES
cal: Pruritus. Prophylaxis, chronic treatment of asthma.
Prevention of exercise-induced broncho-
ADVERSE EFFECTS/TOXIC constriction. Relief of symptoms of seasonal
REACTIONS allergic rhinitis (hay fever), perennial aller-
Acute hypersensitivity reaction (urticaria, gic rhinitis. OFF-LABEL: Urticaria.
angioedema, severe bronchospasm) occurs
rarely. Transfer from systemic to local ste- PRECAUTIONS
roid therapy may unmask previously sup- Contraindications: Hypersensitivity to mon-
pressed bronchial asthma condition. telukast. Cautions: Systemic corticosteroid

underlined – top prescribed drug


montelukast 795
treatment reduction during montelukast breast milk (do not add to any other liq-
therapy. Concomitant use of CYP3A4 induc- uid or food). • Give within 15 min of
ers. Not for use in acute asthma attacks. opening packet.
ACTION INDICATIONS/ROUTES/DOSAGE
Binds to cysteinyl leukotriene recep- Bronchial Asthma
tors, inhibiting effects of leukotrienes on PO: ADULTS, ELDERLY, CHILDREN 15 YRS
bronchial smooth muscle. Therapeutic AND OLDER: One 10-mg tablet daily,
Effect: Decreases bronchoconstriction, taken in the evening. CHILDREN 6–14
vascular permeability, mucosal edema, YRS: One 5-mg chewable tablet daily,
mucus production. taken in the evening. CHILDREN 2–5
YRS: One 4-mg chewable tablet or oral
PHARMACOKINETICS granules daily, taken in the evening. CHIL-
Route Onset Peak Duration DREN 6–23 MOS: 4 mg (oral granules)
PO N/A N/A 24 hrs once daily in the evening.
PO (chewable) N/A N/A 24 hrs
Seasonal Allergic Rhinitis
Rapidly absorbed from GI tract. Protein PO: ADULTS, ELDERLY, CHILDREN 15 YRS
binding: 99%. Extensively metabolized in AND OLDER: One 10-mg tablet, taken
liver. Excreted almost exclusively in feces. in the evening. CHILDREN 6–14 YRS: One
Half-life: 2.7–5.5 hrs (slightly longer 5-mg chewable tablet, taken in the eve-
in elderly). ning. CHILDREN 2–5 YRS: One 4-mg chew- M
able tablet, or oral granules taken in the
LIFESPAN CONSIDERATIONS evening.
Pregnancy/Lactation: Unknown if dis-
tributed in breast milk. Use during Perennial Allergic Rhinitis
pregnancy only if necessary. Children/ PO: ADULTS, ELDERLY, CHILDREN 15
Elderly: No age-related precautions YRS AND OLDER: One 10-mg tablet,
noted in pts older than 6 yrs or the taken in the evening. CHILDREN 6–14
elderly. YRS: One 5-mg chewable tablet, taken
in the evening. CHILDREN 2–5 YRS: One
INTERACTIONS 4-mg chewable tablet or oral gran-
DRUG: None significant. HERBAL: None ules, taken in the evening. CHILDREN
significant. FOOD: None known. LAB 6–23 MOS: 4 mg oral granules, taken
VALUES: May increase serum ALT, AST, in the evening.
eosinophils.
Exercise-Induced Bronchoconstriction
AVAILABILITY (Rx) Prevention
PO: ADULTS, ELDERLY, CHILDREN 15 YRS
Oral Granules: 4 mg per packet. Tab-
lets: 10 mg. Tablets, Chewable: 4 mg,
AND OLDER: 10 mg 2 or more hrs before
5 mg. exercise. No additional doses within 24
hrs. CHILDREN 6–14 YRS: 5 mg (chew tab)
ADMINISTRATION/HANDLING 2 or more hrs prior to exercise. No addi-
PO
tional doses within 24 hrs.
• May take without regard to food. Dosage in Renal/Hepatic Impairment
When treating asthma, administer in eve- No dose adjustment.
ning. • When treating allergic rhinitis,
may individualize administration SIDE EFFECTS
times. • Granules may be given directly ADULTS, CHILDREN 15 YRS AND OLDER:
in mouth or mixed with carrots, rice, Frequent (18%): Headache. Occa-
applesauce, ice cream, baby formula, or sional (4%): Influenza. Rare (3%–2%):

Canadian trade name Non-Crushable Drug High Alert drug


796 morphine
Abdominal pain, cough, dyspep- j BLACK BOX ALERT jRisk of se-
sia, dizziness, fatigue, dental pain. vere adverse effects when epidural
CHILDREN 6–14 YRS: Rare (less than route of administration is used.
Ingestion of alcohol with morphine
2%): Diarrhea, laryngitis, pharyngitis, ER may increase risk of overdose.
nausea, otitis media, sinusitis, viral Risk of opioid addiction, abuse, and
infection. misuse. Serious, life-threatening,
or fatal respiratory depression
ADVERSE EFFECTS/TOXIC may occur. Prolonged use during
REACTIONS pregnancy may result in neonatal
opioid withdrawal syndrome. Ac-
Suicidal ideation and behavior, depres- cidental ingestion of even one dose
sion have been noted. may result in a fatal overdose. Con-
comitant use with benzodiazepines,
NURSING CONSIDERATIONS other CNS depressants may result
in profound sedation, respiratory
BASELINE ASSESSMENT depression, coma, or death.
Chewable tablet contains phenylalanine Do not confuse morphine with
(component of aspartame); parents HYDROmorphone, or morphine
of phenylketonuric pts should be in- sulfate with magnesium sulfate,
formed. Assess lung sounds for wheez- MS Contin with OxyCONTIN.
ing. Assess for allergy symptoms. Ques- MSO4 and MS are error-prone
tion history of depression, suicidal abbreviations.
M ideation.
FIXED-COMBINATION(S)
INTERVENTION/EVALUATION Embeda: morphine/naloxone (an
Monitor rate, depth, rhythm, type of res- opioid antagonist): 20 mg/0.8 mg, 30
pirations; quality/rate of pulse. Assess mg/1.2 mg, 50 mg/2 mg, 60 mg/2.4
lung sounds for wheezing. Monitor for mg, 80 mg/3.2 mg, 100 mg/4 mg.
change in mood, behavior.
uCLASSIFICATION
PATIENT/FAMILY TEACHING
PHARMACOTHERAPEUTIC: Opi-
• Increase fluid intake (decreases oid agonist (Schedule II). CLINI-
lung secretion viscosity). • Take as CAL: Opioid analgesic.
prescribed, even during symptom-free
periods as well as during exacerba-
tions of asthma. • Do not alter/stop USES
other asthma medications. • Drug is Relief of moderate to severe, acute, or
not for treatment of acute asthma at- chronic pain; analgesia during labor,
tacks. • Report increased use or fre- pain due to MI, dyspnea from pulmo-
quency of short-acting bronchodila- nary edema not resulting from chemical
tors, changes in behavior, suicidal respiratory irritant. Infumorph: Use in
ideation. devices for managing intractable chronic
pain. Extended-Release: Use only when
repeated doses for extended periods of
time are required around the clock.
morphine PRECAUTIONS
mor-feen Contraindications: Hypersensitivity to
(Arymo ER, Duramorph, Infumorph, morphine. Acute or severe asthma, GI
Kadian, M-Eslon , Mitigo, MS obstruction, known or suspected para-
Contin, MS-IR ) lytic ileus, concurrent use of MAOIs or use
of MAOIs within 14 days, severe respira-
tory depression. Extreme Caution: COPD,

underlined – top prescribed drug


morphine 797
cor pulmonale, hypoxia, hypercapnia, tremors, hyperactive reflexes, fever, vom-
preexisting respiratory depression, head iting, diarrhea, yawning, sneezing,
injury, increased ICP, severe hypotension. seizures). Children: Paradoxical excite-
Cautions: Biliary tract disease, pancre- ment may occur; those younger than 2
atitis, Addison’s disease, cardiovascular yrs are more susceptible to respiratory
disease, morbid obesity, adrenal insuffi- depressant effects. Elderly: Paradoxical
ciency, elderly, hypothyroidism, urethral excitement may occur. Age-related renal
stricture, prostatic hyperplasia, debili- impairment may increase risk of urinary
tated pts, pts with CNS depression, toxic retention.
psychosis, seizure disorders, alcoholism.
INTERACTIONS
ACTION DRUG: Alcohol, other CNS depres-
Binds with opioid receptors within CNS, sants (e.g., LORazepam, gabapentin,
inhibiting ascending pain pathways. zolpidem) may increase CNS effects,
Therapeutic Effect: Alters pain per- respiratory depression, hypotension.
ception, emotional response to pain. MAOIs (e.g., phenelzine, selegi-
line) may produce serotonin syndrome.
PHARMACOKINETICS (Reduce dosage to one-fourth of usual
Route Onset Peak Duration morphine dose.) HERBAL: Herbals with
Oral solution 30 min 1 hr 3–5 hrs sedative properties (e.g., chamomile,
Tablets 30 min 1 hr 3–5 hrs kava kava, valerian) may increase CNS
Tablets N/A 3–4 hrs 8–12 hrs depression. FOOD: None known. LAB VAL- M
(extended- UES: May increase serum amylase, lipase.
release)
IV Rapid 0.3 hr 3–5 hrs AVAILABILITY (Rx)
IM 5–30 0.5–1 hr 3–5 hrs
min 2 mg/mL, 4 mg/mL,
Injection Solution:
Epidural 15–60 1 hr 12–20 5 mg/mL, 10 mg/mL. Injection Solution
min hrs (Epidural, Intrathecal, IV Infusion): (Dura-
SQ 10–30 1.1–5 3–5 hrs morph): 0.5 mg/mL, 1 mg/mL. Injection
min hrs Solution, Epidural or Intrathecal: (Infu-
Rectal 20–60 0.5–1 hr 3–7 hrs morph): 10 mg/mL, 25 mg/mL. Injection
min
Solution: (Mitigo): 10 mg/mL, 25 mg/
Variably absorbed from GI tract. Readily mL. Injection Solution, Patient-Controlled
absorbed after IM, SQ administration. Analgesia (PCA) Pump: 1 mg/mL. Solu-
Protein binding: 20%–35%. Widely dis- tion, Oral: 10 mg/5 mL, 20 mg/5 mL, 20
tributed. Metabolized in liver. Primarily mg/mL. Suppository: 5 mg, 10 mg, 20
excreted in urine. Removed by hemodi- mg, 30 mg. Tablets: 15 mg, 30 mg.
alysis. Half-life: 2–4 hrs (increased in Capsules, Extended-Release: 45 mg,
hepatic disease). 75 mg, 90 mg, 120 mg. Capsules, Sus-
tained-Release: 10 mg, 20 mg, 30 mg,
LIFESPAN CONSIDERATIONS 50 mg, 60 mg, 80 mg, 100 mg. Tablets,
Pregnancy/Lactation: Crosses placenta. Extended-Release: 15 mg, 30 mg, 60 mg,
Distributed in breast milk. May prolong 100 mg, 200 mg. Tablets, Extended-Release
labor if administered in latent phase of (Abuse Deterrent): 15 mg, 30 mg, 60 mg.
first stage of labor or before cervical
dilation of 4–5 cm has occurred. Respi- ADMINISTRATION/HANDLING
ratory depression may occur in neonate IV
if mother received opiates during labor.
Regular use of opiates during pregnancy Reconstitution • May give undiluted.
may produce withdrawal symptoms in • For IV injection, may dilute in Sterile
neonate (irritability, excessive crying, Water for Injection or 0.9% NaCl to

Canadian trade name Non-Crushable Drug High Alert drug


798 morphine
final concentration of 1–2 mg/mL. INDICATIONS/ROUTES/DOSAGE
• For continuous IV infusion, dilute to b ALERT c Dosage should be titrated to
concentration of 0.1–1 mg/mL in D5W desired effect.
and give through controlled infusion de-
vice. Analgesia
Rate of administration • Always ad- PO: (Immediate-Release): ADULTS,
minister very slowly. Rapid IV increases risk ELDERLY: 10–30 mg q4h as needed.
of severe adverse reactions (apnea, chest CHILDREN 6 MOS AND OLDER WEIGH-
wall rigidity, peripheral circulatory collapse, ING 50 KG OR MORE: 15–20 mg
cardiac arrest, anaphylactoid effects). q3–4h as needed. CHILDREN 6 MOS
Storage • Store at room temperature. AND OLDER WEIGHING LESS THAN 50
KG: 0.2–0.5 mg/kg q3–4h as needed.
IM, SQ CHILDREN YOUNGER THAN 6 MOS: (Oral
• Administer slowly, rotating injection Solution): 0.08–0.1 mg/kg q3–4h as
sites. • Pts with circulatory impairment needed.
experience higher risk of overdosage due b ALERT c For the Avinza dosage be-
to delayed absorption of repeated admin- low, be aware that this drug is to be ad-
istration. ministered once daily only.
b ALERT c For the Kadian dosage in-
PO
formation below, be aware that this drug
• May give without regard to food.
is to be administered q12h or once daily.
M • Mix liquid form with fruit juice to im-
b ALERT c Be aware that pediatric dos-
prove taste. • Do not break, crush, dis-
ages of extended-release preparations of
solve, or divide extended-release capsule,
Kadian and AVINza have not been estab-
tablets. • Avinza, Kadian: May mix
lished.
with applesauce immediately prior to ad-
b ALERT c For the MS Contin dosage
ministration.
information below, be aware that the
Rectal daily dosage is divided and given q8h or
• If suppository is too soft, chill for 30 q12h.
min in refrigerator or run cold water PO: (Extended-Release [Avinza]):
over foil wrapper. • Moisten supposi- ADU­LTS, ELDERLY: Dosage requirement
tory with cold water before inserting well should be established using prompt-
into rectum. release formulations and is based on total
daily dose. AVINza is given once daily only.
IV INCOMPATIBILITIES PO: (Extended-Release [Kadian]):
Amphotericin B complex (Abelcet, AmBi- ADULTS, ELDERLY: Dosage requirement
some, Amphotec), cefepime (Maxipime), should be established using prompt-release
doxorubicin (Doxil), phenytoin (Dilantin). formulations and is based on total daily
dose. Dose is given once daily or divided
IV COMPATIBILITIES and given q12h.
Amiodarone (Cordarone), atropine, PO: (Extended-Release [MS Con-
bumetanide (Bumex), bupivacaine (Mar- tin]): ADULTS, ELDERLY: Dosage require-
caine, Sensorcaine), dexmedetomidine ment should be established using
(Precedex), dilTIAZem (Cardizem), diphen- prompt-release formulations and is
hydrAMINE (Benadryl), DOBUTamine based on total daily dose. Daily dose is
(Dobutrex), DOPamine (Intropin), glyco- divided and given q8h or q12h.
pyrrolate (Robinul), heparin, hydrOXYzine IV: ADULTS, ELDERLY: 2.5–5 mg
(Vistaril), lidocaine, LORazepam (Ativan), q3–4h as needed. Note: Repeated
magnesium, midazolam (Versed), milrinone doses (e.g., 1–2 mg) may be given
(Primacor), nitroglycerin, potassium, pro- more frequently (e.g., every hr) if
pofol (Diprivan). needed. CHILDREN WEIGHING 50 KG
underlined – top prescribed drug
morphine 799
OR MORE: Initially, 2–5 mg q2–4h ADVERSE EFFECTS/TOXIC
as needed.CHILDREN WEIGHING LESS REACTIONS
THAN 50 KG: Initially, 0.05 mg/kg. Overdose results in respiratory depres-
Range: 0.1–0.2 mg/kg q2–4h as sion, skeletal muscle flaccidity, cold/
needed. NEONATES: Initially, 0.05–0.1 clammy skin, cyanosis, extreme drowsi-
mg/kg/dose q4–6h as needed. ness progressing to seizures, stupor,
IV continuous infusion: ADULTS, coma. Tolerance to analgesic effect,
ELDERLY: 0.8–10 mg/hr. Range: 20–50 mg/ physical dependence may occur with
hr. CHILDREN WEIGHING 50 KG OR MORE: 1.5 repeated use. Prolonged duration of
mg/hr. CHILDREN WEIGHING LESS THAN action, cumulative effect may occur in
50 KG: Initially, 0.01 mg/kg/hr. Range: those with hepatic/renal impairment.
0.01–0.04 mg/kg/hr (10–40 mcg/kg/ Antidote: Naloxone (see Appendix J for
hr). NEONATES: Initially, 0.01 mg/kg/hr dosage).
(10 mcg/kg/hr). Maximum: 0.015–0.02
mg/kg/hr. NURSING CONSIDERATIONS
Patient-Controlled Analgesia (PCA) BASELINE ASSESSMENT
IV: ADULTS, ELDERLY: Usual concen- Pt should be in recumbent position be-
tration: 1 mg/mL. Demand dose: 1 fore drug is given by parenteral route.
mg (range: 0.5–2.5 mg). Lockout inter- Assess onset, type, location, duration
val: 5–10 min. of pain. Obtain vital signs before giving
medication. If respirations are 12/min or M
Dosage in Renal Impairment less (20/min or less in children), with-
Creatinine hold medication, contact physician. Ef-
Clearance Dose fect of medication is reduced if full pain
10–50 mL/min, 75% of normal dose recurs before next dose.
CRRT
Less than 10 mL/ 50% of normal dose INTERVENTION/EVALUATION
min, HD, PD Monitor vital signs 5–10 min after IV
administration, 15–30 min after SQ,
Dosage in Hepatic Impairment IM. Be alert for decreased respirations,
No dose adjustment. B/P. Check for adequate voiding. Moni-
tor daily pattern of bowel activity, stool
SIDE EFFECTS consistency; avoid constipation. Initiate
b ALERT c Ambulatory pts, pts not in deep breathing, coughing exercises, par-
severe pain may experience nausea, ticularly in those with pulmonary impair-
vomiting more frequently than pts in ment. Assess for clinical improvement;
supine position or who have severe record onset of pain relief. Consult physi-
pain. Frequent: Sedation, decreased cian if pain relief is not adequate.
B/P (including orthostatic hypoten- PATIENT/FAMILY TEACHING
sion), diaphoresis, facial flushing, con-
• Discomfort may occur with injec-
stipation, dizziness, drowsiness, nausea,
tion. • Change positions slowly to avoid
vomiting. Occasional: Allergic reaction
orthostatic hypotension. • Avoid tasks
(rash, pruritus), dyspnea, confusion,
that require alertness, motor skills until
palpitations, tremors, urinary retention,
response to drug is established. • Avoid
abdominal cramps, vision changes, dry
alcohol, CNS depressants. • Tolerance,
mouth, headache, decreased appetite,
dependence may occur with prolonged use
pain/burning at injection site.
of high doses. • Report ineffective pain
Rare: Paralytic ileus.
control, constipation, urinary retention.

Canadian trade name Non-Crushable Drug High Alert drug


800 moxifloxacin
Therapeutic Effect: Interferes with
moxifloxacin bacterial DNA replication. Prevents/
delays emergence of resistant organisms.
mox-i-flox-a-sin Bactericidal.
(Avelox, Moxeza, Vigamox)
j BLACK BOX ALERT jMay PHARMACOKINETICS
increase risk of tendonitis, tendon
rupture (increased with concurrent Well absorbed from GI tract after PO
corticosteroids, organ transplant administration. Protein binding: 50%.
recipients, those older than 60 yrs). Widely distributed throughout body
May aggravate myasthenia gravis with tissue concentration often exceed-
(avoid use). ing plasma concentration. Metabolized
Do not confuse Avelox with in liver. Excreted in urine (20%), feces
Avonex. (25%) unchanged. Half-life: PO: 12
uCLASSIFICATION hrs; IV: 15 hrs.
PHARMACOTHERAPEUTIC: Fluoroqui- LIFESPAN CONSIDERATIONS
nolone. CLINICAL: Antibacterial, anti-
biotic. Pregnancy/Lactation: May be dis-
tributed in breast milk. May produce
teratogenic effects. Children: Safety and
USES efficacy not established. Elderly: No
Treatment of susceptible infections age-related precautions noted.
M
due to S. pneumoniae, S. pyogenes, S.
aureus, H. influenzae, M. catarrhalis, INTERACTIONS
K. pneumoniae, M. pneumoniae, C. DRUG: Antacids, iron preparations,
pneumoniae including acute bacterial sucralfate may decrease absorption.
exacerbation of chronic bronchitis, acute NSAIDs (e.g., ibuprofen, ketorolac,
bacterial sinusitis, intra-abdominal infec- naproxen) may increase risks of CNS
tion, community-acquired pneumonia, stimulation/seizures. HERBAL: None sig-
uncomplicated skin/skin structure infec- nificant. FOOD: None known. LAB VAL-
tions. Ophthalmic: Topical treatment of UES: None significant.
bacterial conjunctivitis due to susceptible
strains of bacteria. AVAILABILITY (Rx)
Injection Infusion: 400 mg (250
PRECAUTIONS mL). Ophthalmic Solution: (Moxeza,
Contraindications: Hypersensitivity to moxi- Vigamox): 0.5%. Tablets: 400 mg.
floxacin, other quinolones. Cautions: Renal/
hepatic impairment, bradycardia, acute
ADMINISTRATION/HANDLING
myocardial ischemia, myasthenia gravis, dia- IV
betes, rheumatoid arthritis, seizures, pts with
prolonged QT interval, medications known to Reconstitution • Available in ready-
prolong QT interval, hypokalemia, hypomag- to-use containers.
nesemia, elderly, pts with suspected CNS dis- Rate of administration • Give by IV
order, pts at risk for tendon rupture, tendonitis infusion only. • Avoid rapid or bolus IV
(e.g., renal failure, concomitant use of corti- infusion. • Infuse over 60 min.
costeroids; solid organ transplant recipient,
elderly). Storage • Store at room tempera-
ture. • Do not refrigerate.
ACTION
PO
Inhibits two enzymes, topoisomerase II • Give without regard to food. • Oral
and IV, in susceptible microorganisms. moxifloxacin should be administered 4
underlined – top prescribed drug
moxifloxacin 801
hrs before or 8 hrs after antacids, multi- drop 3 times/day for 7 days. (Mox-
vitamins, iron preparations, sucralfate, eza): 1 drop 2 times/day for 7 days.
didanosine chewable/buffered tablets,
pediatric powder for oral solution. Dosage in Renal Impairment
No dose adjustment.
Ophthalmic
• Place gloved finger on lower eyelid Dosage in Hepatic Impairment
and pull out until a pocket is formed be- Mild to moderate impairment: No dose
tween eye and lower lid. • Place pre- adjustment. Severe impairment: Use
scribed number of drops into caution.
pocket. • Instruct pt to close eye gently
(so medication will not be squeezed out SIDE EFFECTS
of the sac) and to apply digital pressure Frequent (8%–6%): Nausea, diarrhea. Oc-
to lacrimal sac at inner canthus for 1 min casional: PO, IV (3%–2%): Dizziness,
to minimize systemic absorption. headache, abdominal pain, vomiting.
Ophthalmic (6%–1%): Conjunctival
IV INCOMPATIBILITIES irritation, reduced visual acuity, dry eye,
Do not add or infuse other drugs simul- keratitis, eye pain, ocular itching, swell-
taneously through the same IV line. Flush ing of tissue around cornea, eye dis-
line before and after use if same IV line is charge, fever, cough, pharyngitis, rash,
used with other medications. rhinitis. Rare (1%): Altered taste, dyspep-
sia, photosensitivity. M
INDICATIONS/ROUTES/DOSAGE
Usual Dose
ADVERSE EFFECTS/TOXIC
PO, IV: ADULTS, ELDERLY: 400 mg q24h. REACTIONS
Duration dependent on severity of infection. Pseudomembranous colitis (severe abdom-
inal cramps/pain, severe watery diarrhea,
Acute Bacterial Sinusitis fever) may occur. Superinfection (anal/
PO, IV: ADULTS, ELDERLY: 400 mg q24h genital pruritus, moderate to severe diar-
for 10 days. rhea, stomatitis) may occur. May increase
risk of tendonitis, tendon rupture, periph-
Acute Bacterial Exacerbation of Chronic eral neuropathy.
Bronchitis
PO, IV: ADULTS, ELDERLY: 400 mg q24h NURSING CONSIDERATIONS
for 5 days.
BASELINE ASSESSMENT
Community-Acquired Pneumonia Obtain serum BUN, creatinine; CrCl,
PO, IV: ADULTS, ELDERLY: 400 mg q24h GFR in pts with renal impairment; LFT
for 7–14 days. in pts with hepatic impairment. Obtain
bacterial culture and sensitivity prior to
Intra-abdominal Infection administration. Question pt’s usual stool
PO, IV: ADULTS, ELDERLY: 400 mg q24h characteristics (color, frequency, consis-
for 5–14 days. tency). Question medical history as listed
in Precautions, esp. cardiac conduction
Skin/Skin Structure Infection
disorders, CNS disorders, hypersensitivity
PO, IV: ADULTS, ELDERLY: 400 mg once reaction.
daily for 7–21 days.
INTERVENTION/EVALUATION
Topical Treatment of Bacterial
Monitor for CNS reactions (agitation,
Conjunctivitis Due to Susceptible Strains
anxiety, convulsions, depression, hallu-
of Bacteria
cinations, increased ICP, insomnia, night-
Ophthalmic: ADULTS, ELDERLY, CHIL-
mares, suicidal ideation and behavior),
DREN 1 YR AND OLDER: (Vigamox): 1

Canadian trade name Non-Crushable Drug High Alert drug


802 mycophenolate
peripheral neuropathy; hypersensitivity
reactions (throat and facial edema, dys- mycophenolate
pnea, urticaria, itching, hemodynamic
instability); muscle weakness, voice dys- mye-koe-fen-o-late
tonia in pts with myasthenia gravis; pain, (CellCept, Myfortic)
swelling, bruising, popping of tendons. j BLACK BOX ALERT jIncreased
Be alert for superinfections. Obtain ECG risk of congenital malformation,
spontaneous abortion. Increased
if cardiac arrhythmia suspected or pal- risk for development of lymphoma,
pitations occur. Observe daily pattern skin malignancy. Increased sus-
of bowel activity, stool consistency (in- ceptibility to infections. Administer
creased severity may indicate antibiotic- under supervision of physician
associated colitis). If frequent diarrhea experienced in immunosuppressive
therapy.
occurs, obtain C. difficile toxin screen
and initiate isolation precautions until uCLASSIFICATION
test result confirmed. Antibacterial drugs
PHARMACOTHERAPEUTIC: Immu-
that are not directed against C. difficile
infection may need to be discontinued. nologic agent. CLINICAL: Immuno-
Monitor I&O. suppressant.

PATIENT/FAMILY TEACHING
USES
• It is essential to complete drug therapy
M despite symptom improvement. Early dis- Should be used concurrently with other
continuation may result in antibacterial immunosuppressants CellCept: Prophy-
resistance or increase risk of recurrent laxis of organ rejection in pts receiving
infection. • Report any episodes of diar- allogeneic hepatic/renal/cardiac transplant.
rhea, esp. during the first few mos after Myfortic: Renal transplants. OFF-LABEL:
final dose. Frequent diarrhea, fever, ab- Treatment of hepatic transplant rejection in
dominal pain, blood-streaked stool may pts unable to tolerate tacrolimus or cyclo-
indicate infectious diarrhea, which may be SPORINE due to toxicity, mild heart trans-
contagious to others. • Severe allergic plant rejection, moderate to severe psoriasis,
reactions, such as hives, palpitations, rash, proliferative lupus nephritis, myasthenia
shortness of breath, swelling of tongue, gravis, graft-vs-host disease. Treatment of
may occur. • Tendon inflammation/ autoimmune hepatitis (refractory).
swelling, tendon rupture may occur; re-
PRECAUTIONS
port bruising, pain, swelling in tendon ar-
eas or snapping, popping of ten- Contraindications: Hypersensitivity to myco-
dons. • Immediately report nervous phenolate, mycophenolic acid or polysor-
system problems such as anxiety, confu- bate 80 (IV formulation). Cautions: Active
sion, dizziness, nervousness, nightmares, severe GI disease, renal impairment, neutro-
thoughts of suicide, seizures, tremors, penia, women of childbearing potential (use
trouble sleeping. • Treatment may cause caution when handling).
heart problems such as low heart rate,
ACTION
palpitations; permanent nerve damage
such as burning, numbness, tingling, Suppresses immunologically mediated
weakness. • Do not take aluminum- or inflammatory response by inhibiting
magnesium-containing antacids, multivita- inosine monophosphate dehydrogenase,
mins, zinc or iron products at least 2 hrs an enzyme that deprives lymphocytes
before or 6 hrs after dose. • Drink of nucleotides necessary for DNA, RNA
plenty of fluids. synthesis, thus inhibiting proliferation
of T and B lymphocytes. Therapeutic
Effect: Prevents transplant rejection.

underlined – top prescribed drug


mycophenolate 803

PHARMACOKINETICS ADMINISTRATION/HANDLING
Rapidly, extensively absorbed after PO IV
administration (food decreases drug
plasma concentration but does not affect Reconstitution • Reconstitute each
absorption). Protein binding: 97%. Com- 500-mg vial with 14 mL D5W. Gently agi-
pletely hydrolyzed to active metabolite tate. • For 1-g dose, further dilute with
mycophenolic acid. Primarily excreted 140 mL D5W; for 1.5-g dose, further di-
in urine. Not removed by hemodialysis. lute with 210 mL D5W, providing a con-
Half-life: 17.9 hrs. centration of 6 mg/mL.
Rate of administration • Infuse over
LIFESPAN CONSIDERATIONS at least 2 hrs. • Begin infusion within 4
Pregnancy/Lactation: Unknown if hrs of reconstitution.
drug crosses placenta or is distributed Storage • Store at room temperature.
in breast milk. Breastfeeding not recom-
mended. Increased risk of miscarriage, PO
birth defects. Effective contraception • Give on empty stomach (1 hr before or
should be used during treatment and 2 hrs after food). • Do not break, crush,
for 6 wks after discontinuation. Chil- or open capsules or break, crush, dissolve,
dren: Safety and efficacy not estab- or divide delayed-release tablets. Avoid in-
lished in children younger than 3 months. halation of powder in capsules, direct con-
Elderly: Age-related renal impairment tact of powder on skin/mucous mem-
may require dosage adjustment. branes. If contact occurs, wash thoroughly, M
with soap, water. Rinse eyes profusely with
INTERACTIONS plain water. • May store reconstituted
DRUG: May increase concentration/ suspension in refrigerator or at room tem-
effect of acyclovir, ganciclovir. perature. • Suspension is stable for 60
Antacids (aluminum- and magne- days after reconstitution. • Suspension
sium-containing), cholestyramine can be administered orally or via an NG
may decrease absorption. Live virus tube (minimum size 8 French).
vaccines may potentiate virus repli- IV INCOMPATIBILITIES
cation, increase vaccine side effects,
decrease pt’s antibody response to Mycophenolate is compatible only with
vaccine. Rifampin may decrease con- D5W. Do not infuse concurrently with
centration/effect. May decrease thera- other drugs or IV solutions.
peutic effect of oral contraceptives. INDICATIONS/ROUTES/DOSAGE
HERBAL: Echinacea may decrease
therapeutic effect. FOOD: All foods Prevention of Renal Transplant Rejection
may decrease concentration. LAB VAL- PO, IV: (Cellcept): ADULTS, ELDERLY: 1 g
UES: May increase serum cholesterol, twice daily. PO: CHILDREN 3 MONTHS AND
alkaline phosphatase, creatinine, ALT, OLDER: (Cellcept Suspension): 600 mg/
AST. May alter serum glucose, lipids, m2/dose twice daily. (Tablets, Capsules):
calcium, potassium, phosphate, uric BSA greater than or equal to 1.5 m2:
acid. 1,000 mg twice daily. BSA 1.25–1.5 m2: 750
mg twice daily. Maximum: 1 g twice daily.
AVAILABILITY (Rx) PO: (Myfortic): ADULTS, ELDERLY: 720
Capsules: (CellCept): 250 mg. Injection, mg twice daily. CHILDREN 5–16 YRS: 400
Powder for Reconstitution: (CellCept): 500 mg/m2 twice daily. BSA greater than
mg. Oral Suspension: (CellCept): 200 mg/ 1.58 m2: 720 mg twice daily. BSA 1.19–
mL. Tablets: (CellCept): 500 mg. 1.58 m2: 540 mg twice daily. Maxi-
mum: 720 mg twice daily.
Tablets, Delayed-Release: (Myfor-
tic): 180 mg, 360 mg.
Canadian trade name Non-Crushable Drug High Alert drug
804 mycophenolate
Prevention of Heart Transplant Rejection Immunosuppression results in increased
PO, IV: (Cellcept): ADULTS, ELDERLY: 1.5 susceptibility to infection.
g twice daily in combination with cyclo-
sporine and initially with corticosteroids; NURSING CONSIDERATIONS
or, 1 g twice daily in combination with BASELINE ASSESSMENT
other immunosuppressants (e.g., tacro-
limus, everolimus, or sirolimus). Women of childbearing potential should
have a negative serum or urine pregnancy
Prevention of Hepatic Transplant test within 1 wk before initiation. Assess
Rejection medical history, esp. renal function, exis-
PO, IV: (Cellcept): ADULTS, ELDERLY: 1.5 tence of active digestive system disease,
g twice daily in combination with cyclo- drug history, esp. other immunosuppres-
sporine and initially with corticosteroids; sants.
or, 1 g twice daily in combination with INTERVENTION/EVALUATION
other immunosuppressants (e.g., tacro-
limus, everolimus, or sirolimus). CBC should be performed wkly during
first mo of therapy, twice monthly dur-
Dosage in Renal/Hepatic Impairment ing second and third mos of treatment,
No dose adjustment. then monthly throughout the first yr. If
rapid fall in WBC occurs, dosage should
SIDE EFFECTS be reduced or discontinued. Assess par-
Frequent (37%–20%): UTI, hypertension, ticularly for delayed bone marrow sup-
M pression. Report any major change in
peripheral edema, diarrhea, constipa-
tion, fever, headache, nausea. Occa- assessment of pt.
sional (18%–10%): Dyspepsia, dyspnea,
PATIENT/FAMILY TEACHING
cough, hematuria, asthenia, vomiting,
edema, tremors, oral candidiasis, acne; • Effective contraception should be
abdominal, chest, back pain. Rare (9%– used before, during, and for 6 wks after
6%): Insomnia, respiratory tract infec- discontinuing therapy, even if pt has a
tion, rash, dizziness. history of infertility, other than hysterec-
tomy. • Two forms of contraception
ADVERSE EFFECTS/TOXIC must be used concurrently unless absti-
REACTIONS nence is absolute. • Report unusual
Significant anemia, leukopenia, throm- bleeding/bruising, sore throat, mouth
bocytopenia, neutropenia, leukocytosis sores, abdominal pain, fever. • Labora-
may occur, particularly in pts undergo- tory follow-up while taking medication is
ing renal transplant rejection. Sepsis, important part of therapy. • Malignan-
infection occur occasionally. GI tract cies may occur.
hemorrhage occurs rarely. There is an
increased risk of developing neoplasms.

underlined – top prescribed drug


nafcillin 805
AVAILABILITY (Rx)
nafcillin Injection, Powder for Reconstitution: 1 g,
2 g. Infusion, Premix: 1 g/50 mL, 2g/100
naf-sil-in mL.
uCLASSIFICATION
ADMINISTRATION/HANDLING
PHARMACOTHERAPEUTIC: Penicil- b ALERT c Space doses evenly around
lin. CLINICAL: Antibiotic. the clock.
IV
USES
Reconstitution • Reconstitute each
Treatment of respiratory tract, skin/skin vial with 10 mL Sterile Water for Injection
structure infections, osteomyelitis, endo- or 0.9% NaCl. • For intermittent IV
carditis, meningitis; perioperatively, esp. infusion (piggyback), further dilute with
in cardiovascular, orthopedic proce- 50–100 mL 0.9% NaCl or D5W.
dures. Predominant treatment of infec- Rate of administration • Infuse over
tions caused by susceptible strains of 30–60 min. • Because of potential for
staphylococci. hypersensitivity/anaphylaxis, start initial
dose at few drops per min, increase
PRECAUTIONS
slowly to ordered rate; stay with pt first
Contraindications: Hypersensitivity to 10–15 min, then check q10min. • Limit
nafcillin, other penicillins. Cautions: His- IV therapy to less than 48 hrs, if possible.
tory of allergies, particularly cephalospo- Stop infusion if pt complains of pain at
rins; severe renal/hepatic impairment, IV site. N
asthma, pts with HF. Storage • Refrigerate diluted solution
for up to 7 days or store at room tem-
ACTION
perature for up to 24 hrs. • Discard if
Binds to bacterial membranes. Thera- precipitate forms.
peutic Effect: Inhibits cell wall synthe-
sis. Bactericidal. IM
• Reconstitute each 500 mg with 1.7 mL
LIFESPAN CONSIDERATIONS Sterile Water for Injection or 0.9% NaCl
Pregnancy/Lactation: Readily crosses to provide concentration of 250 mg/
placenta; appears in cord blood, amni- mL. • Inject IM into large muscle
otic fluid. Distributed in breast milk. mass.
May lead to rash, diarrhea, candidiasis
in neonate, infant. Children: Imma- IV INCOMPATIBILITIES
ture renal function in neonate may delay Aztreonam (Azactam), dilTIAZem (Cardi-
renal excretion. Elderly: Age-related zem), droperidol (Inapsine), fentaNYL,
renal impairment may require dosage gentamicin, insulin, labetalol (Normo-
adjustment. dyne, Trandate), methylPREDNISolone
(Solu-Medrol), midazolam (Versed),
INTERACTIONS nalbuphine (Nubain), vancomycin (Van-
DRUG: High doses (2 g q4h) may decrease cocin), verapamil (Isoptin).
effects of warfarin. May decrease effects
of BCG (intravesical), axitinib, bosuti- IV COMPATIBILITIES
nib, cobimetinib, elbasvir, grazopre- Acyclovir, famotidine (Pepcid), fluco-
vir, neratinib, olaparib, ranolazine, nazole (Diflucan), heparin, HYDRO-
sonidegib. HERBAL: None significant. morphone (Dilaudid), lidocaine, lipids,
FOOD: None known. LAB VALUES: May magnesium, morphine, potassium chlo-
cause false-positive Coombs’ test. ride, propofol (Diprivan).

Canadian trade name Non-Crushable Drug High Alert drug


806 nalbuphine
INDICATIONS/ROUTES/DOSAGE PATIENT/FAMILY TEACHING
Usual Dosage • Continue antibiotic for full length of
IV: ADULTS, ELDERLY: 0.5–2 g q4–6h. treatment. • Doses should be evenly
CHILDREN: Mild to Moderate Infec- spaced. • Discomfort may occur with
tions: 100–150 mg/kg/day in divided IM injection. • Report IV discomfort
doses q6h. Maximum: 4 g/day. Severe immediately. • Report diarrhea, rash,
Infections: 150–200 mg/kg/day in other new symptoms.
divided doses q4–6h. Maximum: 12
g/day. NEONATES: 25 mg/kg/dose in
divided doses q6–12h. Dose based on
body weight and postnatal age.
nalbuphine
Dosage in Renal/Hepatic Impairment
No dose adjustment. nal-bue-feen
(Nubain )
SIDE EFFECTS
Frequent: Mild hypersensitivity reaction uCLASSIFICATION
(fever, rash, pruritus), GI effects (nausea, PHARMACOTHERAPEUTIC: Opioid
vomiting, diarrhea). Occasional: Hypo- partial agonist. CLINICAL: Opioid
kalemia with high IV dosages, phlebitis, analgesic.
thrombophlebitis (common in elderly).
Rare: Extravasation with IV administration.
USES
N ADVERSE EFFECTS/TOXIC Relief of moderate to severe pain. OFF-
REACTIONS LABEL: Opioid-induced pruritus.
Potentially fatal antibiotic-associated coli-
tis, superinfections (abdominal cramps, PRECAUTIONS
severe watery diarrhea, fever) may result Contraindications: Hypersensitiv-
from altered bacterial balance in GI tract. ity to nalbuphine. Severe respiratory
Hematologic effects (esp. involving plate- depression, acute or severe bronchial
lets, WBCs), severe hypersensitivity reac- asthma, GI obstruction including para-
tions, anaphylaxis occur rarely. lytic ileus. Cautions: Hepatic/renal
impairment, respiratory depression,
NURSING CONSIDERATIONS recent MI, recent biliary tract impair-
BASELINE ASSESSMENT ment, pancreatitis, hypovolemia, head
Question for history of allergies, esp. trauma, increased intracranial pres-
penicillins, cephalosporins. sure (ICP), pregnancy, pts suspected
of being opioid dependent, obesity, thy-
INTERVENTION/EVALUATION roid dysfunction, prostatic hyperplasia,
Hold medication, promptly report rash urinary stricture, adrenal insufficiency,
(possible hypersensitivity), diarrhea (fe- cardiovascular disease, elderly pts,
ver, abdominal pain, mucus/blood in stool debilitated pts.
may indicate antibiotic-associated colitis).
Evaluate IV site frequently for phlebitis ACTION
(heat, pain, red streaking over vein), in- Agonist of kappa opioid receptors and
filtration (potential extravasation). Moni- partial antagonist of mu opioid receptors
tor periodic CBC, urinalysis, BMP, LFT. Be within CNS, inhibiting ascending pain
alert for superinfection: fever, vomiting, pathways. Therapeutic Effect: Alters
diarrhea, anal/genital pruritus, oral muco- pain perception, emotional response to
sal changes (ulceration, pain, erythema). pain.

underlined – top prescribed drug


nalbuphine 807

PHARMACOKINETICS IM/SQ
Route Onset Peak Duration
• Rotate injection sites. • Administer
undiluted.
IV 2–3 min 2–3 min 3–4 hrs
IM Less than 30 min 3–6 hrs IV INCOMPATIBILITIES
15 min
SQ Less than N/A 3–6 hrs Amphotericin B complex (Abelcet, AmBi-
15 min some, Amphotec), cefepime (Maxipime),
ketorolac (Toradol), nafcillin (Nafcil),
Well absorbed after IM, SQ adminis- piperacillin and tazobactam (Zosyn).
tration. Metabolized in liver. Primarily
eliminated in feces by biliary secretion. IV COMPATIBILITIES
Half-life: 3.5–5 hrs. Dexmedetomidine (Precedex), diphen-
hydrAMINE (Benadryl), droperidol
LIFESPAN CONSIDERATIONS (Inapsine), glycopyrrolate (Robinul),
Pregnancy/Lactation: Readily crosses hydrOXYzine (Vistaril), lidocaine, mid-
placenta. Distributed in breast milk. azolam (Versed), prochlorperazine
Breastfeeding not recommended. May (Compazine), propofol (Diprivan).
cause fetal, neonatal adverse effects dur-
ing labor/delivery (e.g., fetal bradycar- INDICATIONS/ROUTES/DOSAGE
dia). Children: Paradoxical excitement Analgesia
may occur. Pts younger than 2 yrs more IV, IM, SQ: ADULTS, ELDERLY: 10 mg
susceptible to respiratory depression. q3–6h as needed. Do not exceed maxi-
Elderly: More susceptible to respi- mum single dose of 20 mg or daily dose of
ratory depression. Age-related renal 160 mg. CHILDREN 1 YR AND OLDER: 0.1– N
impairment may increase risk of urinary 0.2 mg/kg q3–4h as needed. Maxi-
retention. mum: 20 mg/dose, 160 mg/day.
INTERACTIONS Dosage in Renal/Hepatic Impairment
DRUG: Alcohol, other CNS depres- Use caution.
sants (e.g., LORazepam, morphine,
zolpidem) may increase CNS depres- SIDE EFFECTS
sion. HERBAL: Herbals with sedative Frequent (36%): Sedation. Occasional
properties (e.g., chamomile, kava (9%–3%): Diaphoresis, cold/clammy skin,
kava, valerian) may increase CNS nausea, vomiting, dizziness, vertigo, dry
depression. FOOD: None known. LAB mouth, headache. Rare (less than 1%):
VALUES: May increase serum amylase, Restlessness, emotional lability, paresthe-
lipase. sia, flushing, paradoxical reaction.
AVAILABILITY (Rx) ADVERSE EFFECTS/TOXIC
Injection Solution: 10 mg/mL, 20 mg/mL. REACTIONS
Abrupt withdrawal after prolonged use may
ADMINISTRATION/HANDLING produce symptoms of narcotic withdrawal
IV (abdominal cramping, rhinorrhea, lacri-
mation, anxiety, fever, piloerection [goose
Reconstitution • May give undiluted. bumps]). Overdose results in severe
Rate of administration • For IV respiratory depression, skeletal muscle
push, administer each 10 mg over flaccidity, cyanosis, extreme drowsiness
3–5 min. progressing to seizures, stupor, coma. Tol-
Storage • Store parenteral form at erance to analgesic effect, physical depen-
room temperature. dence may occur with chronic use.

Canadian trade name Non-Crushable Drug High Alert drug


808 naldemedine

NURSING CONSIDERATIONS PRECAUTIONS


Contraindications: Hypersensitivity to na­l-
BASELINE ASSESSMENT demedine. Known or suspected mechani-
Question medical history as listed in cal GI obstruction. Pts at risk of recurrent
Precautions. Obtain vital signs before GI obstruction. Cautions: Severe hepatic
giving medication. If respirations are 12/ impairment, pts with advanced illness as-
min or less (20/min or less in children), sociated with impaired structural integrity
withhold medication, contact physician. of the GI wall or conditions that may im-
Assess onset, type, location, duration of pair integrity of GI wall (e.g., Crohn’s dis-
pain. Effect of medication is reduced if ease, diverticulitis, GI tract malignancies,
full pain recurs before next dose. intestinal adhesions, Ogilvie’s syndrome,
INTERVENTION/EVALUATION
peptic ulcers, peritoneal malignancies).
Concomitant use of strong CYP3A induc-
Monitor for change in respirations, B/P, ers, other opioid antagonists. Pts with
rate/quality of pulse. Monitor daily pat- disruption to the blood-brain barrier
tern of bowel activity, stool consistency. (may precipitate symptoms of opioid
Initiate deep breathing, coughing exer- ­withdrawal).
cises, particularly in pts with pulmonary
impairment. Assess for clinical improve- ACTION
ment, record onset of relief of pain. Blocks opioid binding at the peripheral
Consult physician if pain relief is not mu, delta, and kappa opioid receptors
adequate. in GI tract. Inhibits the delay in GI transit
PATIENT/FAMILY TEACHING times. Therapeutic Effect: Decreases
N constipating effects of opioids.
• Avoid alcohol. • Avoid tasks that re-
quire alertness, motor skills until re- PHARMACOKINETICS
sponse to drug is established. • May
cause dry mouth. • May be habit Widely distributed. Metabolized in liver.
­forming. Protein binding: 93%–94%. Peak plasma
concentration: 45 mins (with food: 2.5
hrs). Excreted in urine (57%), feces
(35%). Not removed by dialysis. Half-
life: 11 hrs.
naldemedine LIFESPAN CONSIDERATIONS
nal-dem-e-deen Pregnancy/Lactation: May cross the
(Symproic) placenta and cause fetal opiate withdrawal
due to immature blood-brain barrier. Due
uCLASSIFICATION to risk of opiate withdrawal in nursing
PHARMACOTHERAPEUTIC: Opioid infants, breastfeeding not recommended
receptor antagonist (peripheral act- during treatment and for at least 3 days
ing) (Schedule II). CLINICAL: GI after discontinuation. Children: Safety
agent. and efficacy not established. Elderly: No
age-related precautions noted.
USES INTERACTIONS
Treatment of opioid-induced constipa- DRUG: P-gp/ABCB1 inhibitors (e.g.,
tion (OIC) in adult pts with chronic non- amiodarone), dilTIAZem, proton pump
cancer pain, including pts with chronic inhibitors (e.g., omeprazole, pan-
pain related to prior cancer or its treat- toprazole), strong CYP3A inhibitors
ment, who do not require frequent (e.g., (e.g., clarithromycin, ketoconazole,
weekly) opioid dosage escalation. ritonavir) may increase concentration/
underlined – top prescribed drug
naldemedine 809
effect; Strong CYP3A inducers (e.g., NURSING CONSIDERATIONS
carBAMazepine, phenytoin, rifAMPin)
may decrease concentration/effect. Meth- BASELINE ASSESSMENT
ylnaltrexone, opioid antagonists may Discontinue all maintenance laxative
increase adverse/toxic effects. HERBAL: therapy prior to initiation. Laxatives
St. John’s wort may decrease concentra- may be restarted if therapy has been
tion/effect. FOOD: None known. LAB VAL- ineffective for 3 days. Changes to anal-
UES: None known. gesic dosage prior to initiation is not
required. Question characteristics of
AVAILABILITY (Rx) constipation, frequency of bowel move-
Tablets: 0.2 mg. ments. Assess bowel sounds. Question
history of GI obstruction, GI perfora-
ADMINISTRATION/HANDLING tion, or baseline GI disease. Receive
PO full medication history, including herbal
• Give with or without food. products, and screen for interactions.
Assess hydration status.
INDICATIONS/ROUTES/DOSAGE
Opioid-Induced Constipation INTERVENTION/EVALUATION
PO: ADULTS, ELDERLY: 0.2 mg once daily. Pts may be less responsive to therapy if
(Discontinue if opioid pain medication is taking opioids for less than 4 wks. Moni-
discontinued.) tor for opioid withdrawal symptoms, esp.
in pts taking methadone or with disrup-
Dosage in Renal Impairment tions to blood-brain barrier. Monitor for
No dose adjustment. severe, persistent, or worsening of ab- N
Dosage in Hepatic Impairment
dominal pain; may indicate GI tract ob-
Mild to moderate impairment: No
struction or perforation. Encourage fluid
dose adjustment. Severe impairment: intake. Monitor daily pattern of bowel
Not recommended. activity, stool consistency. Discontinue
treatment if opioid pain medication is
SIDE EFFECTS also discontinued. If dose is increased to
Frequent (21%–12%): Abdominal pain.
25 mg/day in pts with renal impairment,
Occasional (9%–3%): Diarrhea, nausea, flat-
monitor for adverse effects.
ulence, vomiting, headache, hyperhidrosis. PATIENT/FAMILY TEACHING

ADVERSE EFFECTS/TOXIC • Take with or without food. • Do not


REACTIONS take laxatives unless approved by pre-
scriber. • Notify prescriber if opioid
Severe abdominal pain, diarrhea requir- pain medication is discontinued. • Im-
ing hospitalization have occurred. GI per- mediately report severe, persistent ab-
foration was reported in pts with baseline dominal pain; may indicate tear or
GI disease (Crohn’s disease, diverticuli- blockage in GI tract. • Do not ingest
tis, GI tract malignancies, peptic ulcers, grapefruit products or take herbal sup-
Ogilvie’s syndrome, peritoneal malignan- plements. • Opioid withdrawal may oc-
cies). Symptoms of opiate withdrawal cur in a fetus of pregnant females due to
including abdominal pain, anxiety, chills, undeveloped fetal blood-brain bar-
diarrhea, feeling cold, flushing, hyper- rier. • Do not breastfeed during treat-
hidrosis, increased lacrimation, irrita- ment and for at least 3 days after last
bility, nausea were reported, esp. in pts dose. • Do not take newly prescribed
taking methadone or with disruptions medication unless approved by pre-
to the blood-brain barrier. May increase scriber who originally started treatment.
risk of adverse effects in pts with renal
impairment.
Canadian trade name Non-Crushable Drug High Alert drug
810 naloxegol
than 2 hrs. Excreted in feces (68%),
naloxegol urine (16%). Half-life: 6–11 hrs.
nal-ox-ee-gol LIFESPAN CONSIDERATIONS
(Movantik) Pregnancy/Lactation: Known to cross
Do not confuse naloxegol with the placenta. Use during pregnancy may
naloxone. induce fetal opiate withdrawal due to
immature blood-brain barrier. Unknown if
uCLASSIFICATION
excreted in breast milk. Breastfeeding not
PHARMACOTHERAPEUTIC: Mu-opi- recommended due to risk of opiate with-
oid receptor antagonist (Peripherally drawal in nursing infants. Children: Safety
acting). CLINICAL: GI agent. and efficacy not established. Elderly: No
age-related precautions noted.
INTERACTIONS
USES DRUG: P-gp/ABCB1 inhibitors (e.g.,
Treatment of opioid-induced constipa- amiodarone, cycloSPORINE), dil-
tion (OIC) in adult pts with chronic non- tiazem, PPIs (e.g., pantoprazole),
cancer pain, including pts with chronic moderate CYP3A inhibitors (e.g.,
pain related to prior cancer or its treat- erythromycin, ciprofloxacin, dilTIA-
ment who do not require frequent (e.g., Zem, dronedarone, fluconazole, vera-
weekly) opioid dosage escalation. pamil), strong CYP3A inhibitors (e.g.,
clarithromycin, ketoconazole, rito-
PRECAUTIONS navir) may increase concentration/effect;
N
Contraindications: Hypersensitivity to may increase risk of opiate withdrawal.
naloxegol. Known or suspected mechani- Strong CYP3A inducers (e.g., carBA-
cal GI obstruction, pts at risk for recurrent Mazepine, phenytoin, rifAMPin) may
GI obstruction. Concomitant use of strong decrease concentration/effect. Methyl-
CYP3A inhibitors. Cautions: Moderate to naltrexone, opioid antagonists may
severe renal impairment, end-stage renal increase adverse/toxic effects. HERBAL: St
disease, severe hepatic impairment; pts John’s wort may decrease concentration/
with risk or reduction of structural wall effect. FOOD: Grapefruit products may
integrity of GI tract (e.g., Crohn’s disease, increase concentration/effect. LAB VAL-
diverticulitis, GI tract malignancies, pep- UES: None known.
tic ulcers, Ogilvie’s syndrome, peritoneal
metastases). Pts with disruptions to the AVAILABILITY (Rx)
blood-brain barrier. Concomitant use of Tablets: 12.5 mg, 25 mg.
moderate CYP3A inhibitors, P-glycopro-
tein (P-gp) inhibitors. Avoid concomitant ADMINISTRATION/HANDLING
use of strong CYP3A inducers, other opi- PO
oid antagonists. • Give on empty stomach at least 1 hr
prior to first meal or 2 hrs after first
ACTION meal. • Swallow whole; do not chew.
Blocks opioid binding at peripheral For pts unable to swallow tablet whole,
mu-opioid receptors in GI tract. Thera- tablets may be crushed and mixed with
peutic Effect: Decreases constipating 120 mL water for oral administration or
effects of opioids. mixed with 60 mL for NG tube adminis-
tration. After administration of crushed
PHARMACOKINETICS tablet, refill container with 120 mL
Rapidly absorbed. Widely distributed. (oral) or 60 mL (NG tube) of water, stir
Metabolized in liver. Protein binding: well, and give remaining contents. • Do
4.2%. Peak plasma concentration: less not give with grapefruit products.
underlined – top prescribed drug
naloxegol 811

INDICATIONS/ROUTES/DOSAGE NURSING CONSIDERATIONS


Note: Discontinue all maintenance laxa-
tive therapy prior to use. May reintroduce BASELINE ASSESSMENT
laxatives if suboptimal response to nalox- Discontinue all maintenance laxative
egol after 3 days. therapy prior to initiation. Laxatives may
be restarted if therapy has been ineffec-
Opioid-Induced Constipation tive for 3 days. Changes to analgesic dos-
PO: ADULTS, ELDERLY: 25 mg once daily age prior to initiation are not required.
in am. May reduce dose to 12.5 mg once Question characteristics of constipation,
daily if 25-mg dose is not tolerated. frequency of bowel movements. Assess
bowel sounds. Question history of GI
Dose Modification
obstruction, perforation, baseline GI
Concomitant use of moderate CYP3A
disease. Receive full medication history
inhibitors: 12.5 mg daily in am. Strong
including herbal products and screen for
CYP3A inhibitors: Contraindicated.
interactions. Assess hydration status.
Dosage in Renal Impairment
INTERVENTION/EVALUATION
Mild impairment: No dose adjustment.
Moderate to severe impairment: Pts may be less responsive to therapy if
CrCl less than 60 mL/min: ESRD: taking opioids for less than 4 wks. Moni-
Reduce dose to 12.5 mg once daily in am. tor for opioid withdrawal symptoms, esp.
If tolerated, may increase to 25 mg once in pts taking methadone or with disrup-
daily in am. tions to blood-brain barrier. Monitor for
severe, persistent, worsening of abdomi-
Dosage in Hepatic Impairment nal pain; may indicate GI tract obstruc- N
Mild to moderate impairment: No tion, perforation. Encourage fluid intake.
dose adjustment. Severe impairment: Monitor daily pattern of bowel activity,
Not recommended; avoid use. stool consistency. Discontinue treatment
if opioid pain medication is also discon-
SIDE EFFECTS tinued. If dose is increased to 25 mg/day
Frequent (21%–12%): Abdominal pain. in pts with renal impairment, monitor for
Occasional (9%–3%): Diarrhea, nausea, flat- increased adverse effects.
ulence, vomiting, headache, hyperhidrosis.
PATIENT/FAMILY TEACHING
ADVERSE EFFECTS/TOXIC
• Take on an empty stomach in the am at
REACTIONS
least 1 hr before or 2 hrs after morning
Severe abdominal pain, diarrhea requir- meal. • Do not take laxatives unless
ing hospitalization have occurred. GI per- approved by prescriber. • Tablets may
foration was reported in pts with baseline be taken whole or crushed and mixed in
GI disease (Crohn’s disease, diverticulitis, water. • Notify prescriber if opioid pain
GI tract malignancies, peptic ulcers, Ogil- medication is discontinued. • Immedi-
vie’s syndrome, peritoneal malignancies). ately report severe, persistent abdominal
Symptoms of opiate withdrawal, including pain; may indicate tear or blockage in GI
abdominal pain, anxiety, chills, diarrhea, tract. • Do not ingest grapefruit prod-
hyperhidrosis, irritability, yawning, were ucts or take herbal supplements. • Opi-
reported, esp. in pts taking methadone oid withdrawal may occur in a fetus of
or with disruptions to the blood-brain pregnant females due to undeveloped fe-
barrier. May increase risk of adverse tal blood-brain barrier. • Do not
effects in pts with renal impairment who breastfeed.
have increased dose to 25 mg/day.

Canadian trade name Non-Crushable Drug High Alert drug


812 naloxone

PHARMACOKINETICS
naloxone Route Onset Peak Duration
nal-ox-own IV 1–2 min N/A 20–60 min
IM 2–5 min N/A 20–60 min
(Evzio, Narcan, Narcan Nasal
SQ 2–5 min N/A 20–60 min
Spray)
Do not confuse naloxone with Well absorbed after IM, SQ administration.
Lanoxin or naltrexone. Metabolized in liver. Primarily excreted in
urine. Half-life: 60–100 min.
FIXED-COMBINATION(S)
Embeda: naloxone/morphine (an opi- LIFESPAN CONSIDERATIONS
oid agonist): 0.8 mg/20 mg, 1.2 mg/30 Pregnancy/Lactation: Unknown if
mg, 2 mg/50 mg, 2.4 mg/60 mg, 3.2 drug crosses placenta or is distributed in
mg/80 mg, 4 mg/100 mg. Suboxone breast milk. Children/Elderly: No age-
(sublingual film): naloxone/bu- related precautions noted.
prenorphine (an analgesic): 0.5 mg/2
mg, 1 mg/4 mg, 2 mg/8 mg, 3 mg/12 INTERACTIONS
mg. Zubsolv: naloxone/buprenor- DRUG: Methylnaltrexone may increase
phine: 0.36 mg/1.4 mg, 1.4 mg/ 5.7 mg. adverse/toxic effects. May increase adverse/
toxic effects of naldemedine, naloxegol.
uCLASSIFICATION HERBAL: None significant. FOOD: None
PHARMACOTHERAPEUTIC: Opioid known. LAB VALUES: None significant.
antagonist. CLINICAL: Antidote.
N AVAILABILITY (Rx)
Injection, Autoinjector: (Evzio): 2 mg/0.4
mL. Injection Solution: 0.4 mg/mL, 1 mg/
USES mL. Narcan Nasal Spray: 4 mg/0.1 mL.
Narcan: Complete or partial reversal of
opioid depression including respiratory ADMINISTRATION/HANDLING
depression. Diagnosis of suspected opi- IV
oid tolerance or acute opioid overdose.
Evzio, Narcan Nasal Spray: Emergency Reconstitution • For IV push, may give
treatment of known or suspected opioid undiluted (0.4 mg/mL or diluted with 9
overdose. OFF-LABEL: Opioid-induced mL 0.9% NaCl to concentration of 0.04
pruritus. mg/mL). • For continuous IV infusion,
dilute each 2 mg of naloxone with 500 mL
of D5W or 0.9% NaCl, producing solution
PRECAUTIONS containing 0.004 mg/mL (4 mcg/mL).
Contraindications: Hypersensitivity to Rate of administration • May give IV
naloxone. Cautions: Cardiac/pulmonary push over 30 sec.
disease. Medications with potential for Storage • Store parenteral form at
adverse cardiovascular effects (e.g., room temperature. • Use mixture within
hypotension, arrhythmias). 24 hrs; discard unused solution. • Pro-
tect from light. • Stable in D5W or 0.9%
ACTION NaCl at 4 mcg/mL for 24 hrs.
Displaces opioids at opioid-occupied IM
receptor sites in CNS. Therapeutic • Give deep IM in large muscle mass.
Effect: Reverses opioid-induced sleep/
sedation, increases respiratory rate, IV INCOMPATIBILITIES
raises B/P to normal range. Amphotericin B complex (Abelcet, AmBi-
some, Amphotec).
underlined – top prescribed drug
naproxen 813

IV COMPATIBILITIES increased B/P, tachycardia, seizures.


Heparin, ondansetron (Zofran), propo- Excessive dosage in postoperative pts
fol (Diprivan). may produce significant reversal of anal-
gesia, agitation, tremors. Hypotension or
INDICATIONS/ROUTES/DOSAGE hypertension, ventricular tachycardia/
Note: If no response seen after a total of fibrillation, pulmonary edema may occur
10 mg, consider other causes of respira- in pts with cardiovascular disease.
tory depression.
NURSING CONSIDERATIONS
Opioid Overdose BASELINE ASSESSMENT
IV, IM, SQ: ADULTS, ELDERLY: 0.4–2 mg
Maintain patent airway. Obtain weight of
q2–3min as needed. After reversal, addi-
children to calculate drug dosage.
tional doses may be required at later inter-
vals (e.g., 20–60 min) depending on type/ INTERVENTION/EVALUATION
duration of opioid. CHILDREN 5 YRS AND Monitor vital signs, esp. rate, depth,
OLDER, WEIGHING 20 KG OR MORE: 2 mg/ rhythm of respiration, during and
dose; if no response, may repeat q2–3min. ­frequently following administration. Care-
May need to repeat doses q20–60min. fully observe pt after satisfactory r­ esponse
CHILDREN YOUNGER THAN 5 YRS, WEIGH- (duration of opiate may exceed duration
ING LESS THAN 20 KG: 0.1 mg/kg (Maxi- of naloxone, resulting in ­recurrence of
mum: 2 mg); if no response, repeat respiratory depression). Assess for in-
q2–3min. May need to repeat doses q20– creased pain with reversal of opiate.
60min. (Narcan Nasal Spray): ADULTS,
ELDERLY, CHILDREN: Single spray (4 mg) N
into one nostril. May give q2–3min until
emergency medical assistance arrives. naproxen
(Evzio): IM: ADULTS, ELDERLY, CHILDREN: 2
mg (contents of 1 auto-injector) as a single na-prox-en
dose; may repeat q2–3min until emergency (Aleve, EC-Naprosyn, Naprelan,
medical assistance becomes available. Naprosyn)
j BLACK BOX ALERT j In-
Reversal of Respiratory Depression with creased risk of serious cardiovascu-
Therapeutic Opioid Dosing lar thrombotic events, including my-
IV, IM, SQ: ADULTS, ELDERLY: Initially, ocardial infarction, CVA. Increased
0.02–0.2 mg. Titrate to avoid profound risk of severe GI reactions, including
ulceration, bleeding, perforation of
withdrawal, seizures, arrhythmias, or severe stomach, intestines.
pain. CHILDREN: 0.001–0.015 mg/kg. Do not confuse Aleve with
Titrate to desired effect. If administered IM Alesse, or Anaprox with Anas-
or SQ, dose is to be given in divided doses. paz or Avapro.
Dosage in Renal/Hepatic Impairment
FIXED-COMBINATION(S)
No dose adjustment.
Prevacid NapraPac: naproxen/lan-
SIDE EFFECTS soprazole (proton pump inhibitor):
None known; little or no pharmacologic 375 mg/15 mg, 500 mg/15 mg.
effect in absence of narcotics. Treximet: naproxen/SUMAtriptan (an
antimigraine): 60 mg/10 mg; 500
ADVERSE EFFECTS/TOXIC mg/85 mg. Vimovo: naproxen/esome-
REACTIONS prazole (proton pump inhibitor): 375
Too-rapid reversal of narcotic-induced mg/20 mg, 500 mg/20 mg.
respiratory depression may result in
agitation, nausea, vomiting, tremors,
Canadian trade name Non-Crushable Drug High Alert drug
814 naproxen
uCLASSIFICATION renal impairment may increase risk of
PHARMACOTHERAPEUTIC: NSAID. hepatic/renal toxicity; reduced dosage
CLINICAL: Analgesic, nonopioid. recommended. More likely to have serious
adverse effects with GI bleeding/ulceration.
USES INTERACTIONS
Treatment of acute or long-term mild DRUG: May increase effect of apixa-
to moderate pain, primary dysmenor- ban, dabigatran, edoxaban, riva-
rhea, rheumatoid arthritis (RA), juvenile roxaban. Bile acid sequestrants
rheumatoid arthritis (JRA), osteoarthri- (e.g., cholestyramine) may decrease
tis, ankylosing spondylitis, acute gouty absorption. May increase nephrotoxic
arthritis, bursitis, tendonitis, fever. OFF- effect of aliskiren, cyclosporine.
LABEL: Migraine prophylaxis. HERBAL: Glucosamine, herbals with
anticoagulant/antiplatelet proper-
PRECAUTIONS ties (e.g., garlic, ginger, ginseng,
Contraindications: History of asthma, ginkgo biloba) may increase concen-
urticaria; hypersensitivity to naproxen, tration/effect. FOOD: None known. LAB
other NSAIDs. Perioperative pain in set- VALUES: May prolong bleeding time.
ting of CABG surgery. Cautions: GI disease May increase serum BUN, creatinine, ALT,
(bleeding, ulcers), fluid retention, renal/ AST, alkaline phosphatase. May decrease
hepatic impairment, asthma, HF, concur- Hgb, Hct, leukocytes, platelets, uric acid.
rent use of anticoagulants, smoking, use
of alcohol, elderly pts, debilitated pts. AVAILABILITY (Rx)
N Capsule: 220 mg. Oral Suspension: 125
ACTION mg/5 mL naproxen. Tablets: 220 mg, 250
Reversibly inhibits COX-1 and COX-2 mg, 275 mg, 375 mg, 500 mg, 550 mg.
enzymes, resulting in decreased forma- Tablets, Delayed-Release: 375 mg,
tion of prostaglandin precursors. Thera- 500 mg. Extended-Release: 375 mg, 500
peutic Effect: Reduces inflammatory mg, 750 mg.
response, fever, intensity of pain.
ADMINISTRATION/HANDLING
PHARMACOKINETICS
PO
Route Onset Peak Duration • Give controlled-release form whole. Do
PO (analge- 1 hr 2–4 hrs 7 hrs or not break, crush, dissolve, or divide. • Best
sic) less taken with food or milk (decreases GI irrita-
PO (anti-in- 2 wks 2–4 wks 12 hrs
flammatory)
tion). • Shake suspension well.

Completely absorbed from GI tract. Pro- INDICATIONS/ROUTES/DOSAGE


tein binding: 99%. Metabolized in liver. Note: Dosage expressed as naproxen
Primarily excreted in urine. Not removed base (200 mg naproxen base equivalent
by hemodialysis. Half-life: 13 hrs. to 220 mg naproxen sodium).
LIFESPAN CONSIDERATIONS Rheumatoid Arthritis (RA), Osteoarthritis,
Pregnancy/Lactation: Crosses placenta. Ankylosing Spondylitis
Distributed in breast milk. Avoid use during PO: ADULTS, ELDERLY: (Immediate-
third trimester (may adversely affect fetal Release): 500–1,000 mg/day in 2
cardiovascular system: premature closing divided doses. May increase to 1,500
of ductus arteriosus). Children: Safety and mg/day for limited time (less than 6
efficacy not established in pts younger than mos). (Extended-Release): Initially,
2 yrs. Children older than 2 yrs at increased 750–1,000 mg once daily. May increase
risk for skin rash. Elderly: Age-related temporarily to 1,500 mg once daily.

underlined – top prescribed drug


naratriptan 815
Acute Gouty Arthritis nephrotoxicity (dysuria, hematuria,
PO: ADULTS, ELDERLY: 500 mg twice proteinuria, nephrotic syndrome), and
daily (start within 24–48h of flare-up). severe hypersensitivity reaction (fever,
Discontinue 2–3 days after clinical signs chills, bronchospasm).
resolve. (Usual duration: 5–7 days.)
NURSING CONSIDERATIONS
Mild to Moderate Pain, Dysmenorrhea,
Bursitis, Tendonitis BASELINE ASSESSMENT
PO: ADULTS, ELDERLY: (Immediate- Assess onset, type, location, duration of pain/
Release): Initially, 500 mg, then 500 mg inflammation. Inspect appearance of af-
q12h or 250 mg q6–8h as needed. Max- fected joints for immobility, deformities, skin
imum: 1,250 mg on day 1, then 1,000 condition. Question history of GI bleeding,
mg once daily. (Extended-Release): gastric or duodenal ulcers, hypertension.
Initially, 1,000 mg once daily. May tem-
porarily increase to 1,500 mg once daily, INTERVENTION/EVALUATION
then reduce to 1,000 mg once daily. Assist with ambulation if dizziness occurs.
Periodically monitor renal function test dur-
Juvenile Idiopathic Arthritis (JIA) ing chronic use. Monitor daily pattern of
PO: (Oral Suspension Recom- bowel activity, stool consistency. Evaluate for
mended): CHILDREN OLDER THAN 2 therapeutic response: relief of pain, stiffness,
YRS: 10–15 mg/kg/day in 2 divided swelling; increased joint mobility, reduced
doses. Maximum: 1,000 mg/day. joint tenderness, improved grip strength.
OTC Uses (Pain, Fever) PATIENT/FAMILY TEACHING
PO: ADULTS 65 YRS AND YOUNGER, CHIL- • Avoid tasks that require alertness, mo- N
DREN 12 YRS AND OLDER: Initially, 400 tor skills until response to drug is estab-
mg once, then 200 mg q8–12h. Maxi- lished. • Take with food, milk. • Avoid
mum: 400 mg in any 8- to12-hr period aspirin, alcohol during therapy (in-
or 600 mg/day. ELDERLY: Use with caution creases risk of GI bleeding). • Report
(consider a lower dose). headache, rash, visual disturbances,
weight gain, black or tarry stools, bleed-
Dosage in Renal Impairment ing, persistent headache.
Not recommended with CrCl less than 30
mL/min.
Dosage in Hepatic Impairment
naratriptan
Use caution.
nar-a-trip-tan
SIDE EFFECTS (Amerge)
Do not confuse naratriptan with
Frequent (9%–4%): Nausea, constipa-
eletriptan or almotriptan, or
tion, abdominal cramps/pain, heartburn,
Amerge with Altace or Amaryl.
dizziness, headache, drowsiness. Occa-
sional (3%–1%): Stomatitis, diarrhea, uCLASSIFICATION
indigestion. Rare (less than 1%): Vomit-
PHARMACOTHERAPEUTIC: Seroto-
ing, confusion.
nin receptor agonist. CLINICAL: An-
timigraine.
ADVERSE EFFECTS/TOXIC
REACTIONS
Rare reactions with long-term use include USES
peptic ulcer, GI bleeding, gastritis, severe Treatment of acute migraine headache
hepatic reactions (cholestasis, jaundice), with or without aura in adults.

Canadian trade name Non-Crushable Drug High Alert drug


816 naratriptan

PRECAUTIONS ADMINISTRATION/HANDLING
Contraindications: Hypersensitivity to PO
na­ratriptan. Basilar/hemiplegic migraine, • Give without regard to food. • Do
cerebrovascular disease, peripheral not break, crush, dissolve, or divide tab-
vascular disease, coronary artery dis- lets. Swallow whole with water.
ease, ischemic heart disease (includ-
ing angina pectoris, history of MI, silent INDICATIONS/ROUTES/DOSAGE
ischemia, Prinzmetal’s angina), severe Acute Migraine Attack
hepatic impairment (Child-Pugh Grade PO: ADULTS: 1–2.5 mg. If headache
C), severe renal impairment (CrCl less improves but then returns, dose may
than 15 mL/min), uncontrolled hyper- be repeated after 4 hrs. Maximum: 5
tension, use within 24 hrs of ergotamine- mg/24 hrs.
containing preparations or another Dosage in Renal/Hepatic Impairment
serotonin receptor agonist, 5-HT agonist
Hepatic Creatinine
(e.g., SUMAtriptan), MAOI use within 14
Failure Clearance Dosage
days. Cautions: Mild to moderate renal/
hepatic impairment, pt profile suggesting Mild to 15–39 mL/min Initial, 1 mg;
moderate Max: 2.5
cardiovascular risks, elderly. mg/24 hrs
Severe Less than 15 Contraindi-
ACTION mL/min cated
Binds selectively to serotonin recep-
tors, producing vasoconstrictive effect SIDE EFFECTS
on cranial blood vessels. Therapeutic Nausea. Rare (2%): Par-
N Effect: Relieves migraine headache.
Occasional (5%):
esthesia, dizziness, fatigue, drowsiness,
PHARMACOKINETICS feeling of pressure in throat, neck, jaw.
Well absorbed after PO administration. ADVERSE EFFECTS/TOXIC
Protein binding: 28%–31%. Metabolized REACTIONS
in liver. Eliminated primarily in urine. Corneal opacities, other ocular defects
Half-life: 6 hrs (increased in hepatic/ may occur. Cardiac events (ischemia,
renal impairment). coronary artery vasospasm, MI), non-
cardiac vasospasm-related reactions
LIFESPAN CONSIDERATIONS (hemorrhage, cerebrovascular accident
Pregnancy/Lactation: Unknown if [CVA]) occur rarely, particularly in pts
drug is distributed in breast milk. Chil- with hypertension, diabetes, strong family
dren: Safety and efficacy not established. history of coronary artery disease, obese
Elderly: Not recommended in the elderly. pts, smokers, males older than 40 yrs,
postmenopausal women.
INTERACTIONS
DRUG: Ergotamine-containing medi­ NURSING CONSIDERATIONS
cations may produce vasospastic reaction. BASELINE ASSESSMENT
SSRIs (e.g., escitalopram, paroxetine,
sertraline), SNRIs (e.g., duloxetine, Question medical history as listed in Pre-
venlafaxine) may produce serotonin cautions. Question pt regarding possible
syndrome. HERBAL: None significant. precipitating symptoms, onset, location,
FOOD: None known. LAB VALUES: None duration of migraine.
significant. INTERVENTION/EVALUATION

AVAILABILITY (Rx) Assess for relief of migraine headache;


potential for photophobia, phonophobia
Tablets: 1 mg, 2.5 mg. (sound sensitivity), nausea, vomiting.
underlined – top prescribed drug
necitumumab 817
PATIENT/FAMILY TEACHING PRECAUTIONS
• Do not chew, crush, dissolve, or divide Contraindications: Severe hypersensitiv-
tablet; swallow whole with water. • May ity to necitumumab. Cautions: COPD,
repeat dose after 4 hrs (maximum of 5 chronic arrhythmias, coronary artery dis-
mg/24 hrs). • May cause dizziness, fa- ease, HF, recent MI (within 6 mos), pts at
tigue, drowsiness. • Avoid tasks that risk for electrolyte imbalance (e.g., adre-
require alertness, motor skills until re- nal insufficiency, alcoholism, renal failure,
sponse to drug is established. • Report thyroid disorders, malnutrition, chronic
any chest pain, palpitations, tightness in diarrhea; concomitant use of medication
throat, rash, hallucinations, anxiety, known to cause electrolyte abnormalities);
panic. history of venous or arterial thrombosis
(e.g., CVA, DVT, MI, pulmonary embo-
lism). Not indicated for treatment of non-
squamous non–small-cell lung cancer.
necitumumab
ACTION
ne-si-toom-oo-mab Binds to ligand-binding site of EGFR and
(Portrazza) prevents activation, expression, signaling
j BLACK BOX ALERT jCardiopul- of EGFR. Therapeutic Effect: Inhibits
monary arrest and/or sudden death tumor cell growth and metastasis.
reported in 3% of pts (when treated
in combination with gemcitabine
and cisplatin). Closely monitor PHARMACOKINETICS
serum electrolytes, esp. serum cal- Widely distributed. Metabolism not speci-
cium, magnesium, potassium, and N
fied. Elimination not specified. Half-
aggressively replace as appropri-
ate. Hypomagnesemia occurred in life: 14 days.
83% of pts and was severe in 20%.
Monitor pts for hypomagnesemia, LIFESPAN CONSIDERATIONS
hypocalcemia, hypokalemia prior to Pregnancy/Lactation: Avoid ­pregnancy;
each dose, during treatment, and up may cause fetal harm. Female pts of
to 8 wks after discontinuation. With-
hold treatment for CTCAE Grade 3 reproductive potential should use effec-
or 4 electrolyte abnormality. tive contraception during treatment and
Do not confuse necitumumab for at least 3 mos after discontinuation.
with adalimumab, belimumab, Unknown if distributed in breast milk.
daratumumab, ipilimumab, Breastfeeding not recommended during
nivolumab, ofatumumab, or treatment and up to 3 mos after discon-
panitumumab. tinuation. Children: Safety and efficacy
not established. Elderly: May have
uCLASSIFICATION increased risk of venous thromboembo-
PHARMACOTHERAPEUTIC: Epider- lism (including pulmonary embolism).
mal growth factor receptor (EGFR)
inhibitor. Monoclonal antibody. INTERACTIONS
CLINICAL: Antineoplastic. DRUG: None known. HERBAL: None
known. FOOD: None known. LAB VAL-
UES: May decrease serum calcium, mag-
USES nesium, potassium.
First-line treatment (in combination with
gemcitabine and CISplatin) of metastatic AVAILABILITY (Rx)
squamous non–small-cell lung cancer Injection Solution: 800 mg/50 mL (16
(NSCLC). mg/mL).

Canadian trade name Non-Crushable Drug High Alert drug


818 necitumumab

ADMINISTRATION/HANDLING Infusion Reactions


Any Grade 1 reaction: Decrease rate
IV by 50%. Grade 2 reaction: Interrupt
Preparation • Visually inspect for infusion until resolved to Grade 1 or 0,
particulate matter or discolor- then resume with rate reduced by 50%
ation. • Solution should appear clear for all subsequent infusions. Grade 3
to slightly opalescent, colorless to slightly reaction: Permanently discontinue.
yellow in color. Discard if solution is
cloudy or particulate matter is Dermatological Toxicity
observed. • Dilute in 250 mL 0.9% Grade 3 rash or acneiform rash: With-
NaCl bag. • Do not use solutions con- hold treatment until resolved to Grade 2
taining dextrose. • Gently invert to mix. or better, then reduce dose to 400 mg for
Do not shake or agitate. at least 1 treatment cycle. If tolerated, may
Infusion guidelines • For pts with increase dose to 600 mg and 800 mg for
prior Grade 1 or 2 infusion reaction, subsequent cycles.
premedicate with diphenhydrAMINE (or Permanent discontinuation: Grade
equivalent) before each subsequent infu- 3 rash or acneiform rash that does not
sion. • For pts with recurrent Grade 1 resolve to Grade 2 or better within 6 wks;
or 2 infusion reaction (despite adminis- worsening of skin reaction or intolerance
tration of diphenhydrAMINE), premedi- at 400 mg dose; Grade 3 skin induration
cate with dexamethasone (or equivalent), or fibrosis; Grade 4 dermatologic toxicity.
acetaminophen, diphenhydrAMINE (or
Electrolyte Imbalance
equivalent) before each subsequent infu-
Withhold treatment for any Grade 3 or
N sion. • Once infusion is complete, flush
4 electrolyte abnormalities. Resume
IV line with 0.9% NaCl only.
once abnormalities resolve to Grade 2
Rate of administration • Infuse over
or better.
60 mins using infusion pump via dedi-
cated line. Venous/Arterial Thrombosis
Storage • Refrigerate unused vials in Any occurrence: Permanently discon­
original carton until time of use. • Pro- tinue.
tect from light. • May refrigerate
diluted solution up to 24 hours or at Dosage in Renal Impairment
room temperature up to 4 hrs. No dose adjustment.
IV INCOMPATIBILITIES Dosage in Hepatic Impairment
Do not mix with dextrose-containing Mild to moderate impairment: No
solutions. Do not infuse with other medi- dose adjustment. Severe impairment:
cations or electrolytes. Not specified; use caution.

INDICATIONS/ROUTES/DOSAGE SIDE EFFECTS


Non–Small-Cell Lung Cancer Frequent (44%–29%): Rash, vomiting.
IV: ADULTS, ELDERLY: 800 mg on days Occasional (16%–5%): Diarrhea, derma-
1 and 8 of each 3-wk cycle (in combi- titis acneiform, decreased weight, stoma-
nation with gemcitabine and CISplatin). titis, headache, acne, pruritus, dry skin,
Continue until disease progression or paronychia, conjunctivitis, blurry vision,
unacceptable toxicity. dry eye, reduced visual acuity, blepharitis,
eye pain, increased lacrimation, ocular
Dose Modification hyperemia, visual impairment, eye pruri-
Based on Common Terminology Criteria tus, skin fissures. Rare (3%–1%): Dyspha-
for Adverse Events (CTCAE). gia, muscle spasm, oropharyngeal pain.

underlined – top prescribed drug


necitumumab 819

ADVERSE EFFECTS/TOXIC INTERVENTION/EVALUATION


REACTIONS Diligently monitor serum electrolytes,
All cases were reported in combina- esp. serum magnesium, potassium, cal-
tion with gemcitabine and CISplatin. Pts cium, ionized calcium, during therapy
with severe hypomagnesemia, hypokale- and up to 8 wks after discontinuation.
mia, hypocalcemia are at an increased Monitor for symptoms of hypocalcemia,
risk for cardiac arrhythmias or sudden hypokalemia, hypomagnesemia. Obtain
death. Cardiopulmonary arrest and/ ECG, vital signs if arrhythmia, chest pain,
or sudden death occurred in 3% of palpitations, syncope occurs. Aggres-
pts. Most cases of cardiopulmonary sively replace electrolytes as appropri-
arrest occurred within 30 days of the ate. Pts with sudden chest pain, dyspnea,
last dose and involved co-morbidities hypoxia, tachycardia should be evalu-
including COPD, coronary artery dis- ated for pulmonary embolism. Monitor
ease, hypomagnesemia, hypertension. for symptoms of DVT (leg or arm pain/
Hypomagnesemia reported in 83% of swelling), CVA (aphasia, altered LOC,
pts with median onset of approx. 6 wks. hemiplegia, vision loss, headache, hom-
Severe hypomagnesemia (Grade 3 or 4) onymous hemianopsia [vision loss on the
reported in 20% of pts. Infusion reac- same side of both eyes]), MI (chest pain,
tion (any grade) reported in 1.5% of dyspnea, syncope, diaphoresis, left arm
pts. Life-threatening venous and arterial pain, jaw pain). Monitor for hemoptysis.
thromboembolic events including pul- Assess skin for rash, hypersensitivity re-
monary embolism (5% of pts), DVT (2% action; eyes for infection, subconjunctival
of pts), CVA (2% of pts), MI (1% of pts); hemorrhage.
thrombosis of mesenteric veins, pul- N
PATIENT/FAMILY TEACHING
monary artery/vein, axillary vein, vena
cava, subclavian vein; thrombophlebi- • Therapy may cause low levels of po-
tis may occur. Hemoptysis reported in tassium, magnesium, calcium in the
10% of pts. Ocular toxicities including blood and may be life threatening. Re-
conjunctivitis, conjunctival hemorrhage, place electrolytes exactly as in-
eye infections were reported. Severe skin structed. • Report symptoms of elec-
toxicities occurred in 8% of pts. Immu- trolyte imbalance such as fainting,
nogenicity (auto-necitumumab antibod- fatigue, muscle cramps, palpations, pa-
ies) occurred in 4% of pts. ralysis, numbness or tingling, seizures,
weakness. • Avoid pregnancy; treat-
NURSING CONSIDERATIONS ment may cause birth defects. Female pts
of childbearing potential should use ef-
BASELINE ASSESSMENT fective contraception during treatment
Obtain baseline BMP, serum magnesium, and for at least 3 mos after last dose. Do
ionized calcium; vital signs prior to each not breastfeed during therapy and for at
dose. Obtain pregnancy test in female pts least 3 mos after last dose. • Treatment
of reproductive potential. Receive full may cause blood clots in the arms, legs,
medication history and screen for drugs lungs, brain, heart, or abdomen. Imme-
known to cause electrolyte imbalance. diately report symptoms of stroke (diffi-
Assess nutritional status. Question his- culty speaking, confusion, paralysis, vi-
tory of CVA, DVT, pulmonary embolism, sion loss), heart attack (chest pain,
cardiac disease, recent MI; conditions shortness of breath, fainting, dizziness,
known to cause electrolyte imbalance; profuse sweating, left arm or jaw pain),
prior hypersensitivity reaction to any lung embolism (difficulty breathing, fast
drug in treatment regimen; prior infusion heart rate, chest pain), or blood clots in
reaction. Offer emotional support. Con- the arms or legs (pain/swelling). • Re-
duct full dermatological exam. port skin rashes, allergic reactions,

Canadian trade name Non-Crushable Drug High Alert drug


820 neratinib
coughing up blood; eye problems such PHARMACOKINETICS
as infection, vision impairment, collec- Widely distributed. Metabolized in liver.
tion of blood in the whites of the Protein binding: 99%. Peak plasma con-
eyes. • Avoid sunlight, tanning beds. centration: 2–8 hrs. Excreted in feces
Wear protective clothing, high SPF sun- (97%), urine (1%). Half-life: 7–17 hrs.
screen, and lip balm when outdoors.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Avoid pregnancy;
may cause fetal harm/malformations.
Unknown if distributed in breast milk.
neratinib Breastfeeding not recommended during
treatment and for at least 1 month after
ne-ra-ti-nib last dose. Females of reproductive potential
(Nerlynx) should use effective contraception during
Do not confuse neratinib with treatment and for at least 1 mo after dis-
afatinib, axitinib, bosutinib, continuation. Males: Males with female
cabozantinib, dasatinib, gefitinib, partners of reproductive potential should
imatinib, ponatinib, tofacitinib. use effective contraception during treat-
uCLASSIFICATION ment and up to 3 mos after discontinuation.
Children: Safety and efficacy not estab-
PHARMACOTHERAPEUTIC: Epider- lished. Elderly: May have increased risk of
mal growth factor receptor (EGFR) adverse reactions/toxic effects. Use caution.
inhibitor. Tyrosine kinase inhibitor.
N CLINICAL: Antineoplastic. INTERACTIONS
DRUG: Aluminum-, magnesium-, cal-
cium-containing antacids, H2 receptor
USES antagonists (e.g., famotidine), proton
Extended adjuvant treatment of adult pts pump inhibitors (e.g., omeprazole,
with early stage HER2-overexpressed/ pantoprazole) may decrease concentra-
amplified breast cancer, to follow adju- tion/effect. Strong CYP3A4 inhibitors
vant trastuzumab-based therapy. (e.g., clarithromycin, ketoconazole,
ritonavir), moderate CYP3A inhibitors
PRECAUTIONS (e.g., erythromycin, ciprofloxacin,
Contraindications: Hypersensitivity to dilTIAZem, dronedarone, flucon-
neratinib. Cautions: Dehydration, elec- azole, verapamil) may increase concen-
trolyte imbalance, hepatic impairment, tration/effect. CYP3A4 inducers (e.g.,
irritable bowel syndrome with diarrhea. carBAMazepine, phenytoin, rifAMPin)
Avoid concomitant use of strong or mod- may decrease concentration/effect. May
erate CYP3A inhibitors, CYP3A inducers; increase concentration of pazopanib,
proton pump inhibitors, H2 receptor topotecan. HERBAL: None significant.
antagonists, antacids. FOOD: Grapefruit products may increase
concentration/effect. LAB VALUES: May
ACTION increase serum ALT, AST, bilirubin.
Irreversibly binds to epidermal growth
factor receptor (EGFR), human epider- AVAILABILITY (Rx)
mal growth factor receptor 2 (HER2), Tablets: 40 mg.
HER4, reducing autophosphorylation
and signaling of EGFR and HER2. Thera- ADMINISTRATION/HANDLING
peutic Effect: Exhibits antitumor activ- PO
ity in EGFR and/or HER2 expressing • Give with food. • Administer whole;
cancer cell lines. do not break, cut, crush, or divide
underlined – top prescribed drug
neratinib 821
tablets. • If a dose is missed or vomit- adjust antidiarrheal therapy, diet. Main-
ing occurs after administration, do not tain fluid intake (approx. 2 L/day). If
give extra dose. Administer next dose at diarrhea improves to Grade 1 or 0 within
regularly scheduled time. • Take 3 7 days, resume treatment at same dose
hours after aluminum-, magnesium-, or level. If diarrhea improves to Grade 1
calcium-containing antacids are given. or 0 for more than 7 days, resume treat-
ment at the next reduced dose level. Once
INDICATIONS/ROUTES/DOSAGE improved to Grade 1 or 0, start loperamide
Note: Recommend antidiarrheal pro- 4 mg with each administration. CTCAE
phylaxis during first 2 cycles (56 days) Grade 4 diarrhea (life-threatening
of therapy. event, emergent intervention indi-
cated); recurrent Grade 2 diarrhea (or
Breast Cancer
higher) at 120 mg dose: Permanently
PO: ADULTS, ELDERLY: 240 mg (6 tablets)
once daily for 1 yr. discontinue.

Loperamide (Antidiarrheal) Prophylaxis Hepatotoxicity


Wks 1–2 (days 1–14): 4 mg three CTCAE Grade 3 serum ALT eleva-
times/day. Wks 3–8 (days 15–56): 4 tion (greater than 5–20 times upper
mg twice daily. Wks 9–52 (days limit normal [ULN]) or CTCAE Grade
57–365): 4 mg as needed (do not 3 serum bilirubin elevation (greater
exceed 16 mg/day). than 3–10 times ULN): Withhold treat-
ment until improved to Grade 1 or 0 and
Dose Reduction Schedule (Neratinib) investigate cause. If serum ALT elevation
First dose reduction: 200 mg daily. improves to Grade 1 or 0 within 3 wks, N
Second dose reduction: 160 mg daily. resume treatment at reduced dose level.
Third dose reduction: 120 mg daily. CTCAE Grade 4 serum ALT elevation
Dose Modification (greater than 20 times ULN) or CTCAE
Any CTCAE Grade 3 toxicity: With- Grade 4 serum bilirubin elevation
hold treatment until improved to Grade 1 (greater than 10 times ULN): Perma-
or 0 (or baseline), then resume at the next nently discontinue and investigate cause.
reduced dose level. Any CTCAE Grade Dosage in Renal Impairment
4 toxicity: Permanently discontinue. Not specified; use caution.
Diarrhea Dosage in Hepatic Impairment
CTCAE Grade 1 diarrhea (increase Mild to moderate impairment (Child-
of greater than 4 stools/day over Pugh A or B): No dose adjustment.
baseline); CTCAE Grade 2 diarrhea Severe impairment (Child-Pugh C):
(increase of 4–6 stools/day over Reduce starting dose to 80 mg.
baseline) lasting more than 5 days,
CTCAE Grade 3 diarrhea (increase of SIDE EFFECTS
greater than 7 stools/day over base- Frequent (95%–26%): Diarrhea, nausea,
line, incontinence, hospitalization, abdominal pain, vomiting. Occasional
self-limiting ADLs lasting more than (18%–4%): Rash (erythematous, follicular,
2 days): Adjust antidiarrheal therapy, generalized, pruritic, pustular, maculo-
diet. Maintain fluid intake (approx. 2 L/ papular, papular, dermatitis, dermatitis
day). Once improved to Grade 1 or 0, acneiform, toxic skin eruption), stomatitis,
start loperamide 4 mg with each admin- mouth ulceration, oral mucosal blister-
istration. Any CTCAE grade diarrhea ing, mucosal inflammation, oropharyngeal
with complications (fever, hypoten- pain, oral pain, glossodynia, glossitis, chei-
sion, renal failure, or Grade 3 or 4 litis, decreased appetite, muscle spasm,
neutropenia): Withhold treatment and dyspepsia, nail disorder (paronychia,
Canadian trade name Non-Crushable Drug High Alert drug
822 niCARdipine
onychoclasis, nail discoloration, nail toxic- dration or hospitalization. Take antidiar-
ity, abnormal nail growth, nail dystrophy), rheal medication exactly as prescribed
dry skin, abdominal distention, decreased (goal is 1–2 bowel movements/day).
weight, dehydration. Rare (3%): Dry mouth. Report worsening of diarrhea or dehy-
dration. • Drink plenty of fluids (at
ADVERSE EFFECTS/TOXIC least 2 L/day if severe diarrhea oc-
REACTIONS curs). • Report liver problems such as
Diarrhea reported in 95% of pts. CTCAE bruising; confusion; amber, dark, or-
Grade 3 diarrhea reported in 40% of ange-colored urine; right upper abdomi-
pts. CTCAE Grade 4 diarrhea reported nal pain; yellowing of the skin or
in less than 1% of pts. Median time of eyes. • Treatment may cause fetal
onset of diarrhea was days to wks. Severe harm; avoid pregnancy. • Females of
diarrhea, dehydration, hypotension, childbearing potential should use effec-
renal failure may occur. Hepatotoxicity tive contraception during treatment and
reported in 5%–10% of pts. for at least 1 mo after last dose. Males
with female partners of childbearing po-
NURSING CONSIDERATIONS tential should use effective contraception
during treatment and up to 3 mos after
BASELINE ASSESSMENT last dose. • Do not breast-
Obtain LFT, vital signs. Obtain BMP and feed. • Avoid grapefruit products, Se-
screen for electrolyte imbalance. Confirm ville oranges, starfruit, herbal supple-
HER2-positive status. Obtain pregnancy ments. • Acid-reducing medications
test prior to initiation. Question current may interfere with absorption; avoid use.
N breastfeeding status. Stress the impor- Do not take aluminum-, magnesium-,
tance of antidiarrheal therapy. Question calcium-containing antacids 3 hrs before
history of IBS with chronic diarrhea, or 3 hrs after dose. • Do not take
hepatic impairment. Assess hydration newly prescribed medications unless ap-
status. Question usual bowel movement proved by the prescriber who originally
patterns, stool characteristics. Receive started treatment.
full medication history and screen for in-
teractions. Offer emotional support.
INTERVENTION/EVALUATION
niCARdipine
Monitor LFT monthly for the first 3 mos, nye-kar-di-peen
then q3mos thereafter. Monitor for hepa- (Cardene IV)
totoxicity (abdominal pain, ascites, con- Do not confuse Cardene SR with
fusion, dark-colored urine, jaundice). Cardizem SR or codeine, or
Obtain BMP (note electrolytes) if severe niCARdipine with NIFEdipine or
diarrhea occurs. Ensure compliance of niMODipine.
antidiarrheal therapy. Additional antidiar-
rheal medication may be needed to man- uCLASSIFICATION
age diarrhea despite treatment with lop- PHARMACOTHERAPEUTIC: Calcium
eramide. Monitor daily pattern of bowel channel blocker. Dihydropyridine.
activity, stool consistency. If treatment- CLINICAL: Antianginal, antihyperten­
related toxicities occur, consider referral sive.
to specialist. Monitor I&O. Assess skin,
nails, oral mucosa for toxic reactions.
USES
PATIENT/FAMILY TEACHING PO: Immediate-Release: Treatment of
• Treatment may cause severe diarrhea, chronic stable (effort-associated) angina, hy-
which may lead to life-threatening dehy- pertension. Sustained-Release: Treat­ment
underlined – top prescribed drug
niCARdipine 823
of hypertension. Parenteral: Short-term concentration/effect. Strong CYP3A4
treatment of hypertension when oral therapy inducers (e.g., carbamazepine, phe-
not feasible or desirable. OFF-LABEL: Blood nytoin, rifampin) may decrease con-
pressure control in acute ischemic stroke centration/effect. HERBAL: Herbals with
and intracranial hemorrhage. hypertensive properties (e.g., lico-
rice, yohimbe) or hypotensive prop-
PRECAUTIONS erties (e.g., garlic, ginger, ginkgo
Contraindications: Hypersensitivity to biloba) may alter effects. St. John’s
niCARdipine. Advanced aortic stenosis. wort may decrease concentration/effect.
Cautions: Cardiac/renal/hepatic dysfunc­ FOOD: Grapefruit products may alter
tion, HF, hypertrophic cardiomyopathy absorption. LAB VALUES: None significant.
with outflow tract obstruction, aortic
stenosis, coronary artery disease, portal AVAILABILITY (Rx)
hypertension. Capsules: 20 mg, 30 mg. Infusion, Ready
to Use: 20 mg/200 mL, 40 mg/200 mL.
ACTION Injection Solution: 2.5 mg/mL (10-mL
Inhibits calcium ion movement across cell vial).
membranes of cardiac, vascular smooth ADMINISTRATION/HANDLING
muscle. Therapeutic Effect: Relaxes
coronary vascular smooth muscle. Causes IV
coronary vasodilation, increasing myo- Reconstitution • Dilute 25-mg vial with
cardial oxygen delivery in angina. 240 mL D5W, 0.45% NaCl, or 0.9% NaCl to
provide concentration of 0.1 mg/mL. N
PHARMACOKINETICS Rate of administration • Give by
Route Onset Peak Duration slow IV infusion. • Change IV site q12h
PO 0.5–2 hrs — 8 hrs if administered peripherally.
IV 10 min — 8 hrs or less Storage • Store at room tempera-
ture. • Diluted IV solution is stable for
Rapidly, completely absorbed from GI 24 hrs at room temperature.
tract. Protein binding: 95%. Metabo-
lized in liver. Primarily excreted in urine. PO
Not removed by hemodialysis. Half- • Give without regard to food. • Do
life: 2–4 hrs. not break, crush, or open capsules. Give
whole.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if dis- IV INCOMPATIBILITIES
tributed in breast milk. Children: Safety Ampicillin (Principen), ampicillin/
and efficacy not established. Elderly: Age- sulbactam (Unasyn), cefepime (Maxip-
related renal impairment may require dos- ime), cefTAZidime (Fortaz), furosemide
age adjustment. (Lasix), heparin, sodium bicarbonate.
INTERACTIONS IV COMPATIBILITIES
DRUG: May increase concentration/ DilTIAZem (Cardizem), DOBUTamine
effects of cycloSPORINE, fosphenytoin, (Dobutrex), DOPamine (Intropin), EPI-
phenytoin. Azole antifungals (e.g., NEPHrine, HYDROmorphone (Dilaudid),
ketoconazole, itraconazole) may labetalol (Trandate), LORazepam (Ativan),
increase adverse effects. Strong CYP3A4 midazolam (Versed), milrinone (Prima-
inhibitors (e.g., clarithromycin, cor), morphine, nitroglycerin, norepi-
ketoconazole, ritonavir) may increase nephrine (Levophed), potassium chloride.

Canadian trade name Non-Crushable Drug High Alert drug


824 nicotine

INDICATIONS/ROUTES/DOSAGE duration of anginal pain, precipitating


Chronic Stable Angina factors (exertion, emotional stress).
PO: ADULTS, ELDERLY: Initially, 20 mg INTERVENTION/EVALUATION
3 times/day. Range: 20–40 mg 3 times/
Monitor B/P, heart rate during and fol-
day (allow at least 3 days between dosage
lowing IV infusion. Assess for peripheral
increases).
edema. Assess skin for facial flushing,
Hypertension dermatitis, rash. Question for asthenia,
PO: ADULTS, ELDERLY: Initially, 20 mg headache. Monitor LFT results. Assess
3 times/day. Range: 20–40 mg 3 times/ ECG, pulse for tachycardia.
day (allow at least 3 days between dosage PATIENT/FAMILY TEACHING
increases).
• May take without regard to food.
Acute Hypertension • Sustained-release capsule taken whole;
IV: ADULTS, ELDERLY (GRADUAL B/P do not break, chew, crush, or
DECREASE): Initially, 5 mg/hr. May increase open. • Avoid alcohol, grapefruit prod-
by 2.5 mg/hr q5–15min. Maximum: 15 ucts; limit caffeine. • Report if anginal
mg/hr. After B/P goal is achieved, adjust pain not relieved or if palpitations, short-
dose to maintain desired BP. ness of breath, swelling, dizziness, constipa-
tion, nausea, hypotension occurs. • Avoid
Dosage in Renal Impairment tasks requiring motor skills, alertness until
ADULTS, ELDERLY: PO: Initially, give response to drug is established.
20 mg q8h (30 mg twice daily [sus-
N tained-release capsules]), then titrate.
IV: No dose adjustment. nicotine
Dosage in Hepatic Impairment
ADULTS, ELDERLY: PO: Initially, give 20 nik-o-teen
mg twice daily, then titrate. IV: No dose (Good Sense Nicotine, Habitrol
adjustment. , NicoDerm , NicoDerm CQ,
­Nicorette, Nicotrol, Nicotrol NS,
SIDE EFFECTS Thrive)
Frequent (10%–7%): Headache, facial flush- Do not confuse NicoDerm with
ing, peripheral edema, light-headedness, Nitroderm.
dizziness. Occasional (6%–3%): Asthenia, uCLASSIFICATION
palpitations, angina, tachycardia. Rare (less
than 2%): Nausea, abdominal cramps, dys-
PHARMACOTHERAPEUTIC: Cho-
pepsia, dry mouth, rash. linergic-receptor agonist. CLINI-
CAL: Smoking deterrent.
ADVERSE EFFECTS/TOXIC
REACTIONS
USES
Overdose produces confusion, slurred
speech, drowsiness, marked hypoten- Treatment to aid smoking cessation for
sion, bradycardia. relief of nicotine withdrawal symptoms
(including nicotine craving). OFF-LABEL:
NURSING CONSIDERATIONS Transdermal: Management of ulcerative
colitis.
BASELINE ASSESSMENT
Concurrent therapy with sublingual nitro- PRECAUTIONS
glycerin may be used for relief of anginal Contraindications: Hypersensitivity to
pain. Record onset, type (sharp, dull, nicotine. Cautions: Smoking post-MI
squeezing), radiation, location, intensity, period, severe or worsening angina,

underlined – top prescribed drug


nicotine 825
active temporomandibular joint disease ADMINISTRATION/HANDLING
(gum), pregnancy, hyperthyroidism, Gum
pheochromocytoma, insulin-dependent • Do not swallow. • Chew 1 piece
diabetes, severe renal impairment, when urge to smoke present. • Chew
eczematous dermatitis, oropharyngeal slowly and intermittently for 30
inflammation, esophagitis, peptic ulcer min. • Chew until distinctive nicotine
(delays healing in peptic ulcer disease), taste (peppery) or slight tingling in
coronary artery disease, recent MI, seri- mouth perceived, then stop; when tin-
ous cardiac arrhythmias, vasospastic gling almost gone (about 1 min), repeat
disease, angina, hypertension, hepatic chewing procedure (this allows constant
impairment, use of oral inhaler/nasal slow buccal absorption). • Too-rapid
spray with bronchospastic disease. chewing may cause excessive release of
nicotine, resulting in adverse effects simi-
ACTION
lar to oversmoking (e.g., nausea, throat
Binds to nicotinic-cholinergic receptors irritation).
at the autonomic ganglia, in the adrenal
medulla, at neuromuscular junction, and Inhaler
in the brain, producing stimulating effect • Insert cartridge into mouthpiece.
in the cortex and a rewards effect in • Puff on nicotine cartridge mouthpiece
the limbic system. Therapeutic for 20 min.
Effect: Provides source of nicotine dur-
ing nicotine withdrawal, reduces with- Lozenge
drawal symptoms. • Do not chew or swallow. • Allow to
dissolve slowly (20–30 min). N
PHARMACOKINETICS
Transdermal
Absorbed slowly after transdermal admin- • Apply promptly upon removal from
istration. Protein binding: 5%. Metabo- protective pouch (prevents evaporation,
lized in liver. Excreted primarily in urine. loss of nicotine). • Use only intact
Half-life: 4 hrs. pouch. Do not cut patch. • Apply only
once daily to hairless, clean, dry skin on
LIFESPAN CONSIDERATIONS
upper body, outer arm. • Replace
Pregnancy/Lactation: Distributed in daily; rotate sites; do not use same site
breast milk. Use of cigarettes, nicotine gum within 7 days; do not use same patch
associated with decrease in fetal breathing longer than 24 hrs. • Normal exposure
movements. Children: Not recommended to water (e.g., bathing, swimming)
in this pt population. Elderly: Age-related should not affect patch. • Wash hands
decrease in cardiac function may require with water alone after applying patch
dosage adjustment. (soap may increase nicotine absorp-
tion). • Discard used patch by folding
INTERACTIONS
patch in half (sticky side together), plac-
DRUG: None significant. HERBAL: None ing in pouch of new patch, and throwing
significant. FOOD: None known. LAB VAL- away in such a way as to prevent child or
UES: None significant. pet accessibility. • Patch may contain
conducting metal; remove prior to MRI.
AVAILABILITY (OTC)
Chewing Gum: 2 mg, 4 mg. Inhalation INDICATIONS/ROUTES/DOSAGE
(Nicotrol Inhaler): 10-mg cartridge. Smoking Cessation Aid to Relieve
Lozenges: 2 mg, 4 mg. Nasal Spray Nicotine Withdrawal Symptoms
(Nicotrol NS): 0.5 mg/spray. Transder- PO: (Chewing Gum): ADULTS, ELDERLY:
mal Patch: 7 mg/24 hrs, 14 mg/24 hrs, 2 mg. Use 4 mg in pts who smoke first
21 mg/24 hrs. cigarette within 30 min of waking. Chew 1
Canadian trade name Non-Crushable Drug High Alert drug
826 NIFEdipine
piece of gum when urge to smoke, up to ADVERSE EFFECTS/TOXIC
24/day. Use following schedule: wks 1–6: REACTIONS
q1–2h (at least 9 pieces/day); wks 7–9: Overdose produces palpitations, tachyar-
q2–4h; wks 10–12: q4–8h. rhythmias, seizures, depression, confu-
PO: (Lozenge): sion, diaphoresis, hypotension, rapid/
b ALERT c For pts who smoke the first weak pulse, dyspnea. Lethal dose for
cigarette within 30 min of waking, ad- adults is 40–60 mg. Death results from
minister the 4-mg lozenge; otherwise, respiratory paralysis.
administer the 2-mg lozenge.
ADULTS, ELDERLY: One 4-mg or 2-mg NURSING CONSIDERATIONS
lozenge q1–2h for the first 6 wks (use at
least 9 lozenges/day first 6 wks); 1 loz- BASELINE ASSESSMENT
enge q2–4h for wks 7–9; and 1 lozenge Screen, evaluate those with coronary heart
q4–8h for wks 10–12. Maximum: 1 disease (history of MI, angina pectoris),
lozenge at a time, 5 lozenges/6 hrs, 20 serious cardiac arrhythmias, Buerger’s
lozenges/day. disease, Prinzmetal’s variant angina.
Transdermal:
INTERVENTION/EVALUATION
b ALERT c Apply 1 new patch q24h.
ADULTS, ELDERLY WHO SMOKE 10 CIGARETTES
Monitor smoking habits, B/P, pulse, sleep
OR MORE PER DAY: Follow the guidelines
pattern, skin for erythema, pruritus,
below. Step 1: 21 mg/day for 6 wks. Step burning at application site if transdermal
2: 14 mg/day for 2 wks. Step 3: 7 mg/ system used.
day for 2 wks. ADULTS, ELDERLY WHO SMOKE PATIENT/FAMILY TEACHING
N LESS THAN 10 CIGARETTES PER DAY: Follow
• Follow guidelines for proper applica-
the guidelines below. Step 1: 14 mg/day tion of transdermal system. • Chew
for 6 wks. Step 2: 7 mg/day for 2 wks. gum slowly to avoid jaw ache, maximize
Nasal: ADULTS, ELDERLY: Each dose
benefit. • Report persistent rash, pruri-
(2 sprays, 1 spray in each nostril) = tus that occurs with patch. • Do not
1 mg nicotine. Initially, 1–2 doses/hr. smoke while wearing patch.
Maximum: 5 doses/hr (10 sprays), 40
doses/day (80 sprays). For best results,
take at least 8 doses/day (16 sprays).
Inhaler: (Nicotrol): ADULTS, ELDERLY: NIFEdipine
Initially, 6–16 cartridges per day. Puff
on nicotine cartridge mouthpiece for nye-fed-i-peen
about 20 min as needed. Maximum: 16 (Adalat CC, Adalat XL , Procardia,
cartridges/day. Procardia XL)
Do not confuse NIFEdipine with
Dosage in Renal/Hepatic Impairment niCARdipine or niMODipine, or
No dose adjustment. Procardia XL with Cartia XT.
SIDE EFFECTS uCLASSIFICATION
Frequent: All forms: Hiccups, nausea. PHARMACOTHERAPEUTIC: Calcium
Gum: Mouth/throat soreness. Trans- channel blocker, dihydropyridine.
dermal: Erythema, pruritus, burning CLINICAL: Antianginal, antihyper-
at application site. Occasional: All tensive.
forms: Eructation, GI upset, dry mouth,
insomnia, diaphoresis, irritability. Gum:
Hoarseness. Inhaler: Mouth/throat irri- USES
tation, cough. Rare: All forms: Dizzi- Immediate-/Extended-Release: Treat-
ness, myalgia, arthralgia. ment of angina due to coronary artery

underlined – top prescribed drug


NIFEdipine 827
spasm (Prinzmetal’s variant angina), (e.g., carvedilol, metoprolol) may have
chronic stable angina (effort-associated additive effect. May increase digoxin con-
angina). Extended-Release: Treatment centration, risk of toxicity. Hypokalemia-
of hypertension. OFF-LABEL: Treatment of producing agents (e.g., furosemide,
Raynaud’s phenomenon, pulmonary hyper- other diuretics) may increase risk of
tension, preterm labor, prevention/treat- arrhythmias. HERBAL: Herbals with
ment of high-altitude pulmonary edema. hypertensive properties (e.g., licorice,
yohimbe) or hypotensive properties
PRECAUTIONS (e.g., garlic, ginger, ginkgo biloba) may
Contraindications: Hypersensitivity to NIFE­ alter effects. St. John’s wort may decrease
dipine. ST elevation myocardial infarction concentration/effect. FOOD: Grapefruit
(STEMI). Cautions: Renal/hepatic impair- products may increase risk for flushing,
ment, obstructive coronary disease, HF, headache, tachycardia, hypotension. LAB
severe aortic stenosis, edema, severe left VALUES: May cause positive ANA, direct
ventricular dysfunction, hypertrophic car- Coombs’ test.
diomyopathy, before major surgery, brady-
cardia, concurrent use with beta blockers AVAILABILITY (Rx)
or digoxin, CYP3A4 inhibitors/inducers. Capsules: 10 mg, 20 mg.
Tablets, Extended-Release: 30 mg,
ACTION 60 mg, 90 mg.
Inhibits calcium ion movement across cell
membranes of vascular smooth muscle ADMINISTRATION/HANDLING
and myocardium during depolarization. PO
Therapeutic Effect: Relaxes coronary • Do not break, crush, dissolve, or N
vascular smooth muscle and coronary divide extended-release tablets. • Give
vasodilation, increases myocardial oxygen without regard to food (Adalat CC, Nife-
delivery (angina), reduces peripheral vas- diac CC should be taken on an empty
cular resistance, reduces arterial B/P. stomach). • Grapefruit products may
alter absorption; avoid use.
PHARMACOKINETICS
Rapidly, completely absorbed from Sublingual
GI tract. Protein binding: 92%–98%. • Capsules must be punctured, chewed,
Metabolized in liver. Primarily excreted and/or squeezed to express liquid into
in urine. Not removed by hemodialysis. mouth.
Half-life: 2–5 hrs.
INDICATIONS/ROUTES/DOSAGE
LIFESPAN CONSIDERATIONS Prinzmetal’s Variant Angina, Chronic
Pregnancy/Lactation: Insignificant Stable (Effort-Associated) Angina
amount distributed in breast milk. Chil- PO: (Extended-Release): ADULTS,
dren: Safety and efficacy not established. ELDERLY: Initially, 30–60 mg/day. May
Elderly: Age-related renal impairment increase at 7- to 14-day intervals. Maxi-
may require dosage adjustment. Use mum: 120 mg/day.
lower initial doses and titrate to response.
Hypertension
INTERACTIONS PO: (Extended-Release): ADULTS,
DRUG: Strong CYP3A4 inducers (e.g., ELDERLY: Initially, 30–60 mg/day. May
rifAMPin, PHENobarbital, phenytoin, increase at 7- to 14-day intervals. Maxi-
carBAMazepine) may decrease concen- mum: 90–120 mg/day. CHILDREN 1–17
tration/effects. CYP3A4 inhibitors (e.g., YRS: Initially, 0.2–0.5 mg/kg/day. Maxi-
clarithromycin, ketoconazole) may mum: 3 mg/kg/day or 120 mg/day.
increase concentration. Beta blockers

Canadian trade name Non-Crushable Drug High Alert drug


828 niMODipine
Dosage in Renal/Hepatic Impairment
No dose adjustment. niMODipine
SIDE EFFECTS nye-mode-i-peen
Frequent (30%–11%): Peripheral edema, (Nimotop , Nymalize)
headache, flushed skin, dizziness. j BLACK BOX ALERT jSevere
Occasional (12%–6%): Nausea, shaki- cardiovascular events, including
ness, muscle cramps/pain, drowsi- fatalities, have resulted when cap-
sule contents have been withdrawn
ness, palpitations, nasal congestion, by syringe and administered by IV
cough, dyspnea, wheezing. Rare injection rather than orally or via
(5%–3%): Hypotension, rash, pruri- nasogastric tube.
tus, urticaria, constipation, abdomi- Do not confuse niMODipine
nal discomfort, flatulence, sexual with niCARdipine or NIFEdipine.
dysfunction.
uCLASSIFICATION
ADVERSE EFFECTS/TOXIC PHARMACOTHERAPEUTIC: Calcium
REACTIONS channel blocker, dihydropyridine.
May precipitate HF, MI in pts with cardiac CLINICAL: Cerebral vasospasm agent.
disease, peripheral ischemia. Overdose
produces nausea, drowsiness, confusion,
slurred speech. Antidote: Glucagon (see USES
Appendix J for dosage). Improvement of neurologic deficits due
to cerebral vasospasm following sub-
N NURSING CONSIDERATIONS arachnoid hemorrhage from ruptured
BASELINE ASSESSMENT
intracranial aneurysms.
Concurrent therapy with sublingual PRECAUTIONS
nitroglycerin may be used for relief Contraindications: Hypersensitivity to
of anginal pain. Record onset, type ni­MOD­ipine. Concurrent use with strong
(sharp, dull, squeezing), radiation, CYP3A4 inhibitors (e.g., clarithro-
location, intensity, duration of anginal mycin, voriconazole). Cautions: Pts
pain; precipitating factors (exertion, with cirrhosis, baseline hypotension,
emotional stress). Check B/P for hy- bradycardia.
potension immediately before giving
medication. LIFESPAN CONSIDERATIONS
INTERVENTION/EVALUATION Pregnancy/Lactation: Unknown if drug
Assist with ambulation if light-headed- crosses placenta or is distributed in breast
ness, dizziness occurs. Assess for pe- milk. Children: Safety and efficacy not
ripheral edema. Assess skin for flushing. established. Elderly: Age-related renal
Monitor LFT. Observe for signs/symptoms impairment may require dosage adjust-
of HF. ment. May experience greater hypotensive
response, constipation.
PATIENT/FAMILY TEACHING
• Go from lying to standing slowly. ACTION
• Report palpitations, shortness of Inhibits movement of calcium ions across
breath, pronounced dizziness, nausea, vascular smooth muscle cell membranes.
exacerbations of angina. • Avoid al- Exerts greatest effect on cerebral ­arteries.
cohol; concomitant grapefruit product Therapeutic Effect: Produces favor­
use. able effect on severity of neurologic
deficits due to cerebral vasospasm. May
prevent cerebral vasospasm.

underlined – top prescribed drug


niraparib 829

PHARMACOKINETICS SIDE EFFECTS


Rapidly absorbed from GI tract. Pro- Occasional (6%–2%): Hypotension, periph-
tein binding: 95%. Metabolized in liver. eral edema, diarrhea, headache. Rare (less
Excreted in bile (80%), urine (20%). than 2%): Allergic reaction (rash, urti-
Not removed by hemodialysis. Half- caria), tachycardia, flushing of skin.
life: 1–2 hrs.
ADVERSE EFFECTS/TOXIC
INTERACTIONS REACTIONS
DRUG: Beta blockers (e.g., Overdose produces nausea, weakness,
carvedilol, metoprolol) may have dizziness, drowsiness, confusion, slurred
additive effect, increase depression of speech.
cardiac SA/AV conduction. CYP3A4
inhibitors (e.g., ­ clarithromycin, NURSING CONSIDERATIONS
ketoconazole, ritonavir) increase con- BASELINE ASSESSMENT
centration/effect. CYP3A4 inducers (e.g., Assess level of consciousness, neuro-
carBAMazepine, phenytoin, rifAMPin) logic response, initially and throughout
may decrease concentration/effect. therapy. Monitor baseline LFT. Assess
HERBAL: Herbals with hypertensive
B/P, apical pulse immediately before
properties (e.g., licorice, yohimbe) or drug administration (if pulse is 60/min
hypotensive properties (e.g., garlic, or less or systolic B/P is less than 90
ginger, ginkgo biloba) may alter effects. mm Hg, withhold medication, contact
St. John’s wort may decrease concentra- ­physician).
tion/effect. FOOD: Grapefruit products
may increase concentration, risk of toxicity. INTERVENTION/EVALUATION N
LAB VALUES: None significant. Monitor CNS response, heart rate, B/P
for evidence of hypotension, bradycardia.
AVAILABILITY (Rx) Monitor transcranial Doppler results for
Solution, Oral: (Nymalize): 60 mg/20 mL. evidence of vasospasm.
Capsules: 30 mg.
PATIENT/FAMILY TEACHING
ADMINISTRATION/HANDLING • Do not chew, crush, dissolve, or divide
PO capsules. • Report palpitations, short-
• Administer 1 hr before or 2 hrs after ness of breath, swelling, constipation,
meals. • If pt unable to swallow, place nausea, dizziness. Immediately report
hole in both ends of capsule with 18-gauge headache, blurry vision, confusion (may
needle to extract contents into syringe. indicate vasospasm).
Empty into NG tube; flush tube with 30 mL
water.
INDICATIONS/ROUTES/DOSAGE niraparib
Subarachnoid Hemorrhage
PO: ADULTS, ELDERLY: 60 mg q4h for 21 nye-rap-a-rib
days. Begin within 96 hrs of subarach- (Zejula)
noid hemorrhage. Do not confuse niraparib with
olaparib, neratinib, or rucaparib.
Dosage in Renal Impairment
No dose adjustment. uCLASSIFICATION
PHARMACOTHERAPEUTIC: Poly(ADP-
Dosage in Hepatic Impairment ribose) polymerase (PARP) inhibitor.
PO: ADULTS, ELDERLY: Reduce dose to CLINICAL: Antineoplastic.
30 mg q4h in pts with cirrhosis.

Canadian trade name Non-Crushable Drug High Alert drug


830 niraparib

USES significant. FOOD: None known. LAB


Maintenance treatment of adult pts with VALUES: May increase serum alkaline
recurrent epithelial ovarian, fallopian phosphatase, ALT, AST, creatinine, GGT.
tube, or primary peritoneal cancer who May decrease ANC, Hgb, Hct, leukocytes,
are in a complete or partial response to neutrophils, RBCs; serum potassium.
platinum-based chemotherapy.
AVAILABILITY (Rx)
PRECAUTIONS Capsules: 100 mg.
Contraindications: Hypersensitivity to ni­
ADMINISTRATION/HANDLING
raparib. Cautions: Baseline anemia, leu-
kopenia, neutropenia, thrombocytopenia; PO
history of hypertension, cardiac disease; • Give with or without food. • Admin-
pts at risk for hemorrhage (e.g., history of ister whole; do not break, cut, crush, or
GI bleeding, coagulation disorders, recent open capsules. • If a dose is missed or
trauma; concomitant use of anticoagu- vomiting occurs after administration, do
lants, antiplatelet medication, NSAIDs). not give extra dose. Administer next dose
at regularly scheduled time. • Adminis-
ACTION tration at bedtime may decrease occur-
Inhibits poly(ADP-ribose) polymerase rence of nausea.
(PARP) enzymatic activity, resulting in
INDICATIONS/ROUTES/DOSAGE
DNA damage, apoptosis, and cellular
death. Therapeutic Effect: Induces Recurrent Epithelial Ovarian, Fallopian
cytotoxicity in tumor cell lines with and Tube, Peritoneal Cancer
N without BRCA deficiencies. PO: ADULTS, ELDERLY: 300 mg once
daily, initiated no later than 8 wks after
PHARMACOKINETICS most recent platinum-containing regi-
Well absorbed. Widely distributed. men. Continue until disease progression
Metabolized by carboxylesterase to or unacceptable toxicity.
inactive metabolite. Protein binding: Dose Reduction Schedule
83%. Peak plasma concentration: 3 hrs. First dose reduction: 200 mg daily.
Excreted in urine (48%), feces (39%). Second dose reduction: 100 mg
Half-Life: 36 hrs. daily.
LIFESPAN CONSIDERATIONS Dose Modification
Pregnancy/Lactation: Avoid preg- Note: If acute myeloid leukemia or
nancy; may cause fetal harm/malforma- myelodysplastic syndrome is confirmed,
tions. Unknown if distributed in breast permanently discontinue.
milk. Breastfeeding not recommended
during treatment and up to 1 mo after Anemia, Neutropenia
discontinuation. Females of reproductive ANC less than 1,000 cells/mm3,
potential should use effective contracep- Hgb level less than 8 g/dL: Withhold
tion during treatment and for at least 6 treatment for maximum of 28 days until
mos after discontinuation. May impair ANC improves to greater than or equal to
fertility in males. Children: Safety and 1,500 cells/mm3 or Hgb level improves
efficacy not established. Elderly: No to 9 g/dL or greater, then resume at
age-related precautions noted. reduced dose level. If ANC or Hgb level
does not improve to an acceptable level
INTERACTIONS within 28 days or if dose is already
DRUG: May decrease therapeutic effect reduced to 100 mg/day, permanently
of BCG (intravesical). HERBAL: None discontinue.

underlined – top prescribed drug


niraparib 831
Hematologic Toxicity Requiring dyspnea. Occasional (19%–10%): Myal-
Transfusion gia, back pain, dizziness, dyspepsia,
Platelet count less than or equal to cough, arthralgia, anxiety, dysgeusia,
10,000 cells/mm3: Consider transfu- dry mouth, palpitations, tachycardia,
sion, then resume at reduced dose level. peripheral edema, decreased weight,
depression.
Nonhematologic Toxicity
Any nonhematologic CTCAE Grade ADVERSE EFFECTS/TOXIC
3 or 4 toxicity when prophylactic REACTIONS
treatment is not possible or toxicity Anemia, neutropenia, leukopenia, throm-
persists despite treatment: Withhold bocytopenia are expected responses
treatment for maximum of 28 days until to therapy, but more severe reactions
resolved, then resume at next lower dose including bone marrow failure may result
level. in life-threatening event. Fatal cases of
Any nonhematologic CTCAE Grade acute myeloid leukemia, myelodysplastic
3 or 4 toxicity lasting more than syndrome reported in 1% of pts. Hyper-
28 days with 100 mg/day regi- tension, hypertensive crisis reported in
men: Permanently discontinue. 9% of pts. Infections including bron-
Thrombocytopenia
chitis, conjunctivitis, nasopharyngitis
Platelet count less than 100,000
(23% of pts), urinary tract infection
cells/mm3: First occurrence: With-
(13% of pts) may occur. Epistaxis may
hold treatment for maximum of 28 days occur, esp. in pts with treatment-induced
until improved to greater than or equal to thrombocytopenia.
N
100,000 cells/mm3, then resume at same NURSING CONSIDERATIONS
or reduced dose level. If platelet count
is less than 75,000 cells/mm3, resume BASELINE ASSESSMENT
at reduced dose level. Second occur- Obtain ANC, CBC, BMP, LFT; vital signs.
rence: Withhold treatment for maximum Obtain pregnancy test in females of re-
of 28 days until improved to greater than or productive potential. Question plans of
equal to 100,000 cells/mm3, then resume breastfeeding. Confirm compliance of
at reduced dose level. If platelet count does effective contraception. Question history
not improve to an acceptable level within of cardiac disease, hypertension. Assess
28 days or if dose is already reduced to 100 hydration status. Screen for active infec-
mg/day, permanently discontinue. tion. Offer emotional support.
Dosage in Renal Impairment INTERVENTION/EVALUATION
Mild to moderate impairment: No Monitor ANC, CBC for anemia, leukopenia,
dose adjustment. Severe impairment, neutropenia, thrombocytopenia wkly for
ESRD: Not specified; use caution. first 4 wks, then monthly for 11 mos, then
periodically thereafter. In pts with platelet
Dosage in Hepatic Impairment count less than 10,000 cells/mm3, consider
Mild impairment: No dose adjust- withholding anticoagulant, antiplatelet
ment. Moderate to severe impair- drugs or proceed with transfusion (if ap-
ment: Not specified; use caution. plicable). Monitor for acute myeloid leuke-
SIDE EFFECTS mia, myelodysplastic syndrome (bleeding
or bruising easily, fatigue, frequent infec-
Frequent (74%–20%): Nausea, fatigue, tions, pyrexia, hematuria, melena, weak-
asthenia, constipation, vomiting, ness, weight loss, cytopenias, increased
abdominal pain/distention, insomnia, requirements for blood transfusion).
headache, decreased appetite, rash, Diligently screen for infections. Monitor
mucositis, stomatitis, hypertension, vital signs for arrhythmia, hypertension,
Canadian trade name Non-Crushable Drug High Alert drug
832 nitrofurantoin
t­achycardia. Offer antiemetic if nausea, impairment (CrCl less than 60 mL/
vomiting occurs. Assess skin for rash, toxic min), infants younger than 1 mo due to
reactions. Encourage nutritional intake. risk of hemolytic anemia. Pregnancy at
term, during labor, or delivery, or when
PATIENT/FAMILY TEACHING
onset of labor is imminent. Pts with his-
• Treatment may depress your immune tory of cholestatic jaundice or hepatic
system and reduce your ability to fight impairment with previous nitrofurantoin
infection. Report symptoms of infection therapy. Cautions: Renal impairment,
such as body aches, burning with urina- diabetes, electrolyte imbalance, ane-
tion, chills, cough, fatigue, fever. Avoid mia, vitamin B deficiency, debilitated pts
those with active infection. • Treatment (greater risk of peripheral neuropathy),
may cause severe bone marrow depres- G6PD deficiency (greater risk of hemo-
sion or new-onset myeloid leukemia; re- lytic anemia), elderly pts, prolonged
port bruising, fatigue, fever, frequent in- therapy (may cause pulmonary toxicity).
fections, shortness of breath, weight loss,
bleeding easily, blood in urine or ACTION
stool. • Avoid pregnancy. Females and Inhibits bacterial enzyme systems, inter-
males of childbearing potential should fering with protein synthesis, anaero-
use effective contraception during treat- bic energy metabolism, DNA, RNA,
ment and for at least 6 mos after last and cell wall synthesis. Therapeutic
dose. • Do not breastfeed during treat- Effect: Bactericidal at therapeutic doses.
ment and for at least 1 mo after final
dose. • Treatment may impair fertility PHARMACOKINETICS
N in males. • Dose administration at bed- Microcrystalline form rapidly, completely
time may decrease occurrence of nausea. absorbed; macrocrystalline form more
slowly absorbed. Food increases absorp-
nitrofurantoin tion. Protein binding: 60%. Primarily
concentrated in urine, kidneys. Metabo-
nye-troe-fue-ran-toyn lized in most body tissues. Primarily
(Furadantin, Macrobid, Macro- excreted in urine. Removed by hemodi-
dantin) alysis. Half-life: 20–60 min.
Do not confuse Macrobid with LIFESPAN CONSIDERATIONS
MicroK or Nitro-Bid, or nitro-
furantoin with Neurontin or Pregnancy/Lactation: Readily crosses
nitroglycerin. placenta. Distributed in breast milk. Con-
traindicated at term and during lactation
uCLASSIFICATION when infant suspected of having G6PD
PHARMACOTHERAPEUTIC: Anti- deficiency. Children: No age-related
bacterial. CLINICAL: Antibiotic, UTI precautions noted in pts older than 1
prophylaxis. mo. Elderly: Avoid use. More likely to
develop acute pneumonitis, peripheral
neuropathy. Age-related renal impair-
USES ment may require dosage adjustment.
Prevention/treatment of UTI caused by
susceptible gram-negative, gram-positive INTERACTIONS
organisms, including E. coli, S. aureus, DRUG: Antacids containing magne-
Enterococcus, Klebsiella, Enterobacter. sium trisilicate may decrease absorption.
Probenecid may increase concentration,
PRECAUTIONS risk of toxicity. May decrease effect of
Contraindications:Hypersensitivity to norfloxacin. HERBAL: None significant.
nitrofurantoin. Anuria, oliguria, renal FOOD: None known. LAB VALUES: May

underlined – top prescribed drug


nitroglycerin 833
increase serum ALT, AST, phosphorus. May ADVERSE EFFECTS/TOXIC
decrease Hgb. REACTIONS
Superinfection, hepatotoxicity, periph-
AVAILABILITY (Rx)
eral neuropathy (may be irreversible),
Capsules: (Macrocrystalline [Macro- Stevens-Johnson syndrome, permanent
bid]): 100 mg. Capsules: (Macrocrys- pulmonary impairment, anaphylaxis
talline [Macrodantin]): 25 mg, 50 mg, occur rarely.
100 mg. Oral Suspension: (Microcrys-
talline [Furadantin]): 25 mg/5 mL. NURSING CONSIDERATIONS
ADMINISTRATION/HANDLING BASELINE ASSESSMENT
PO Question for history of asthma. Evaluate
• Give with food, milk to enhance baseline renal function, LFT. Question
absorption, reduce GI upset. • May mix medical history as listed in Precautions,
suspension with water, milk, fruit juice; and screen for contraindications.
shake well. INTERVENTION/EVALUATION
INDICATIONS/ROUTES/DOSAGE Monitor CBC, BMP, LFT; I&O. Monitor
UTI daily pattern of bowel activity, stool con-
PO: (Furadantin, Macrodantin): sistency. Assess skin for rash, urticaria.
ADULTS, ELDERLY: 50–100 mg q6h; treat Be alert for numbness/tingling, esp. of
males for 7 days or females for 5 days. lower extremities (may signal onset of
Maximum: 400 mg/day. CHILDREN, peripheral neuropathy). Observe for
ADOLESCENTS: 5–7 mg/kg/day in divided
signs of hepatotoxicity (fever, rash, ar- N
doses q6h for 7 days or at least 3 days thralgia, hepatomegaly). Monitor respi-
after obtaining sterile urine. Maxi- ratory status, esp. in pts with asthma.
mum: 400 mg/day (100 mg/dose). PATIENT/ FAMILY TEACHING
PO: (Macrobid): ADULTS, ELDERLY, ADO-
• Urine may become dark yellow/
LESCENTS: 100 mg twice daily; treat brown. • Take with food, milk for best
males for 7 days or females for 5 days. results, to reduce GI upset. • Complete
Long-Term Prevention of UTI full course of therapy. • Avoid sun, ul-
PO: ADULTS, ELDERLY: 50–100 mg traviolet light; use sunscreen, wear pro-
at bedtime. CHILDREN OLDER THAN 1 tective clothing. • Report cough, fever,
MONTH: 1–2 mg/kg/day in 2 divided
chest pain, difficulty breathing, numb-
doses. Maximum: 100 mg/day. ness/tingling of fingers, toes. • Rare
occurrence of alopecia is transient.
Dosage in Renal Impairment
Contraindicated in pts with CrCl less than
60 mL/min. nitroglycerin
Dosage in Hepatic Impairment
nye-troe-glis-er-in
No dose adjustment. (GoNitro, Minitran, Nitro-Bid,
SIDE EFFECTS Nitro-Dur, Nitrolingual, NitroMist,
Nitrostat, Rectiv, Trinipatch )
Frequent: Anorexia, nausea, vomiting, Do not confuse Nitro-Bid with
dark urine. Occasional: Abdominal pain, Macrobid or Nicobid, Nitro-
diarrhea, rash, pruritus, urticaria, hyper- Dur with Nicoderm, nitroglyc-
tension, headache, dizziness, drowsiness. erin with nitrofurantoin or
Rare: Photosensitivity, transient alope-
nitroprusside, or Nitrostat with
cia, asthmatic exacerbation in those with Nilstat or Nystatin.
history of asthma.
Canadian trade name Non-Crushable Drug High Alert drug
834 nitroglycerin
uCLASSIFICATION PHARMACOKINETICS
PHARMACOTHERAPEUTIC: Nitrate. Route Onset Peak Duration
CLINICAL: Antianginal, antihyperten- Sublingual 1–3 min 4–8 min 30–60
sive, coronary vasodilator. min
Transling- 2 min 4–10 min 30–60
ual spray min
USES Buccal 2–5 min 4–10 min 2 hrs
Treatment/prevention of angina pectoris. tablet
PO (ex- 20–45 45–120 4–8 hrs
Extended-release, topical forms used for tended- min min
prophylaxis, long-term angina manage- release)
ment. IV form used in treatment of HF, Topical 15–60 30–120 2–12 hrs
acute MI, perioperative hypertension, min min
induction of intraoperative hypoten- Transder- 40–60 60–180 18–24
sion. Rectiv: Treatment of moderate to mal min min hrs
severe pain associated with chronic anal patch
fissure. OFF-LABEL: Short-term man- IV 1–2 min Immedi- 3–5 min
ate
agement of pulmonary hypertension,
esophageal spastic disorders, uterine Well absorbed after PO, sublingual, topi-
relaxation, treatment of sympathomi- cal administration. Metabolized in liver,
metic vasopressor extravasation. by enzymes in bloodstream. Protein bind-
ing: 60%. Excreted in urine. Not removed
PRECAUTIONS by hemodialysis. Half-life: 1–4 min.
Contraindications: Hypersensitivity to
N nitroglycerin. Allergy to adhesives (trans- LIFESPAN CONSIDERATIONS
dermal); concurrent use of sildenafil, Pregnancy/Lactation: Unknown if drug
tadalafil, vardenafil (PDE5 inhibitors). Con- crosses placenta or is distributed in
current use with riociguat. IV: Restrictive breast milk. Children: Safety and effi-
cardiomyopathy, pericardial tamponade, cacy not established. Elderly: More
constrictive pericarditis, increased ICP, susceptible to hypotensive effects. Age-
uncorrected hypovolemia. Sublingual, related renal impairment may require
Rectal: Increased intracranial pressure, dosage adjustment.
severe anemia. Sublingual: Acute cir-
culatory failure or shock, early MI. Cau- INTERACTIONS
tions: Blood volume depletion, severe DRUG: Alcohol, other antihyperten-
hypotension (systolic B/P less than 90 mm sives (e.g., amLODIPine, lisinopril,
Hg), bradycardia (less than 50 beats/min), valsartan), vasodilators may increase
inferior wall MI and suspected right ven- risk of orthostatic hypotension. Concurrent
tricular involvement. use of sildenafil, tadalafil, vardenafil
(PDE5 inhibitors) produces significant
ACTION hypotension. Ergot derivatives (e.g.,
Dilates coronary arteries, improves col- ergotamine) may decrease effect of vaso-
lateral blood flow to ischemic areas dilation. May increase hypotensive effect of
within myocardium. IV form produces riociguat. HERBAL: Herbals with hyper-
peripheral vasodilation. Therapeutic tensive properties (e.g., licorice,
Effect: Decreases myocardial oxygen yohimbe) or hypotensive properties
demand by decreasing preload (LVDP). (e.g., garlic, ginger, ginkgo biloba)
Improves collateral flow to ischemic may alter effects. FOOD: None known. LAB
areas. Rectal: Decreases sphincter tone VALUES: May increase serum methe­
and intra-anal pressure. moglobin, urine catecholamine concen­
trations.

underlined – top prescribed drug


nitroglycerin 835

AVAILABILITY (Rx) or dose-measuring papers. Do not use


Infusion, Premix: 25 mg/250 mL, 50 fingers; do not rub/massage into skin.
mg/250 mL, 100 mg/250 mL. Injection
Transdermal
Solution: 5 mg/mL. Ointment: (Nitro-
• Apply patch on clean, dry, hairless
Bid): 2%. Ointment, Rectal (Rec-
skin of upper arm or body (not below
tiv): 0.4%. Translingual Spray: 0.4 mg/
knee or elbow). • May keep patch on
spray. Transdermal Patch: 0.1 mg/hr, 0.2
when bathing/showering. • Do not cut/
mg/hr, 0.4 mg/hr, 0.6 mg/hr.
trim to adjust dose.
Capsules, Extended-Release: 2.5 mg,
6.5 mg, 9 mg. Tablets, Sublingual: IV INCOMPATIBILITIES
0.3 mg, 0.4 mg, 0.6 mg. Alteplase (Activase), phenytoin (Dilantin).
ADMINISTRATION/HANDLING IV COMPATIBILITIES
b ALERT c Cardioverter/defibrillator Amiodarone (Cordarone), dexmedetomi-
must not be discharged through paddle dine (Precedex), dilTIAZem (Cardizem),
electrode overlying nitroglycerin (trans- DOBUTamine (Dobutrex), DOPamine
dermal, ointment) application. May (Intropin), EPINEPHrine, famotidine
cause burns to pt or damage to paddle (Pepcid), fentaNYL (Sublimaze), furose-
via arcing. mide (Lasix), heparin, HYDROmorphone
IV
(Dilaudid), insulin, labetalol (Trandate),
lidocaine, lipids, LORazepam (Ativan),
Reconstitution • Available in ready- midazolam (Versed), milrinone (Prima-
to-use injectable containers. • Dilute cor), morphine, niCARdipine (Cardene), N
vials in D5W or 0.9% NaCl. Maximum nitroprusside (Nipride), norepinephrine
concentration: 400 mcg/mL. • Use (Levophed), propofol (Diprivan).
glass bottles.
Rate of administration • Use micro- INDICATIONS/ROUTES/DOSAGE
drop or infusion pump. Angina, CAD
Storage • Store at room tempera- Translingual spray: ADULTS, ELDERLY:
ture. • Reconstituted solutions stable 1 spray (0.4 mg) q5min up to 3 doses in
for 48 hrs at room temperature or 7 days response to chest pain. If chest pain fails
if refrigerated. to improve or worsens in 3-5min after 1
dose, call 911.
PO Sublingual: ADULTS, ELDERLY: One tablet
• Do not break, crush, or open (0.3–0.4 mg) under tongue. If chest pain
extended-release capsules. • Do not fails to improve or worsens in 3–5 min, call
shake oral aerosol canister before lin- 911. After the call, may take additional tab-
gual spraying. let. A third tablet may be taken 5 min after
Sublingual
second dose (maximum of 3 tablets).
PO: (Extended-Release): ADULTS,
• Instruct pt to not swallow. • Dissolve
under tongue. • Administer while ELDERLY: 2.5–6.5 mg 3–4 times/day.
seated. • Slight burning sensation Maximum: 26 mg 4 times/day.
Topical: ADULTS, ELDERLY: Initially, 1/2
under tongue may be lessened by placing
tablet in buccal pouch. • Keep sublin- inch upon waking and 1/2 inch 6 hrs later.
gual tablets in original container. May double dose to 1 inch and double
again to 2 inches. Maximum: 2 doses/day
Topical including nitrate-free interval of 10–12 hrs.
• Spread thin layer on clean, dry, hair- Transdermal patch: ADULTS, ELDERLY:
less skin of upper arm or body (not Initially, 0.2–0.4 mg/hr. Maintenance:
below knee or elbow), using applicator 0.4–0.8 mg/hr. Consider patch on for

Canadian trade name Non-Crushable Drug High Alert drug


836 nitroglycerin
12–14 hrs, patch off for 10–12 hrs (pre- d­ uration of anginal pain; precipitating
vents tolerance). factors (exertion, emotional stress). As-
sess B/P, apical pulse before administra-
HF, Acute MI tion and periodically following dose. Pt
IV: ADULTS, ELDERLY: Initially, 5 mcg/ must have continuous ECG monitoring
min via infusion pump. Increase in for IV administration. Rule out right-
5-mcg/min increments at 3- to 5-min sided MI, if applicable (may precipitate
intervals until B/P response is noted or life-threatening hypotension). Receive
until dosage reaches 20 mcg/min, then full medication history, and screen
increase by 10–20 mcg/min q3–5min. for interactions, esp. use of PDE5 in-
Dosage may be further titrated according hibitors. Question medical history and
to clinical, therapeutic response up to screen for contraindications.
400 mcg/min.
INTERVENTION/EVALUATION
Anal Fissure Monitor B/P, heart rate. Assess for facial,
Rectal: ADULTS, ELDERLY: One inch (1.5 neck flushing. Cardioverter/defibrillator
mg) q12h for up to 3 wks. must not be discharged through paddle
electrode overlying nitroglycerin (trans-
Dosage in Renal/Hepatic Impairment dermal, ointment) system (may cause
No dose adjustment. burns to pt or damage to paddle via elec-
trical arcing). Consider NS boluses for
SIDE EFFECTS hypotension.
Frequent: Headache (possibly severe;
N occurs mostly in early therapy, diminishes PATIENT/FAMILY TEACHING
rapidly in intensity, usually disappears dur- • Go from lying to standing slowly.
ing continued treatment), transient flush- • Take oral form on empty stomach
ing of face/neck, dizziness (esp. if pt is (however, if headache occurs during
standing immobile or is in a warm environ- therapy, take medication with meals).
ment), weakness, orthostatic hypotension. • Use spray only when lying down.
Sublingual: Burning, tingling sensation • Dissolve sublingual tablet under
at oral point of dissolution. Ointment: tongue; do not swallow. • Take at first
Erythema, pruritus. Occasional: GI upset. sign of angina. • May take additional
Transdermal: Contact dermatitis. dose q5min if needed up to a total of 3
doses. • If not relieved within 5 min,
ADVERSE EFFECTS/TOXIC contact physician or immediately go to
REACTIONS emergency room. • Do not change
Discontinue drug if blurred vision, dry brands. • Keep container away from
mouth occurs. Severe orthostatic hypo- heat, moisture. • Do not inhale lingual
tension may occur, manifested by syn- aerosol but spray onto or under tongue
cope, pulselessness, cold/clammy skin, (avoid swallowing after spray is adminis-
diaphoresis. Tolerance may occur with tered). • Expel from mouth any re-
repeated, prolonged therapy; minor tol- maining lingual, sublingual, intrabuccal
erance may occur with intermittent use tablet after pain is completely re-
of sublingual tablets. High doses tend to lieved. • Place transmucosal tablets
produce severe headache. under upper lip or buccal pouch (be-
tween cheek and gum); do not chew/
NURSING CONSIDERATIONS swallow tablet. • Avoid alcohol (inten-
BASELINE ASSESSMENT sifies hypotensive effect). If alcohol is
ingested soon after taking nitroglycerin,
Record onset, type (sharp, dull, squeez- possible acute hypotensive episode
ing), radiation, location, intensity, (marked drop in B/P, vertigo,
underlined – top prescribed drug
nivolumab 837
d­iaphoresis, pallor) may occur. • Do and neck. Treatment of locally advanced
not use within 48 hrs of sildenafil, or metastatic urothelial carcinoma with
tadalafil, vardenafil (PDE5 inhibitors); disease progression during or following
may cause acute hypotensive episode. platinum-containing chemotherapy; or
within 12 mos of neoadjuvant or adjuvant
treatment with platinum-containing che-
nivolumab motherapy. Treatment (as a single agent
or in combination with ipilimumab) of
nye-vol-ue-mab microsatellite instability-high (MSI-H)
(Opdivo) or mismatch repair deficient (dMMR)
Do not confuse nivolumab with metastatic colorectal cancer in adults and
denosumab, adalimumab, or children 12 yrs of age and older that has
palivizumab. progressed following treatment with fluo-
ropyrimidine, oxaliplatin and irinotecan.
uCLASSIFICATION Treatment of hepatocellular carcinoma in
PHARMACOTHERAPEUTIC: Anti-PD-1 pts previously treated with sorafenib.
monoclonal antibody. Immune check- PRECAUTIONS
point inhibitor. CLINICAL: Antineo-
plastic. Contraindications: Hypersensitivity to
nivolum­ab. Cautions: Thyroid/pituitary
disease, hepatic/renal impairment, inter-
USES stitial lung disease, electrolyte imbalance.
Treatment of BRAF V600 wild-type unre-
sectable or metastatic melanoma, as a
ACTION N
single agent; BRAF V600 mutation-posi- Binds PD-1 ligands to PD-1 receptor
tive unresectable melanoma, as a single found on T cells, blocking its interac-
agent; unresectable or metastatic mela- tion with the ligands (PD-L1 and PD-L2).
noma, in combination with ipilimumab. Releases PD-1 pathway–mediated inhibi-
Adjuvant treatment of melanoma with tion of immune response (including anti-
involvement of lymph nodes or metastatic tumor immune response). Therapeutic
disease following complete resection. Effect: Inhibits T-cell proliferation and
Treatment of metastatic non–small-cell cytokine production. Inhibits tumor cell
lung cancer (NSCLC) with progression on growth and metastasis.
or after platinum-based chemotherapy.
Treatment of metastatic small-cell lung
PHARMACOKINETICS
cancer (SCLC) in pts with progression Information on metabolism and elimi-
following platinum-based chemotherapy nation is not available. Steady-state
and at least one other line of therapy. concentration reached in 12 wks. Half-
Treatment of advanced renal cell can- life: 26.7 days.
cer (RCC) in pts receiving prior antian-
giogenic therapy. First-line treatment of
LIFESPAN CONSIDERATIONS
advanced previously untreated RCC (in Pregnancy/Lactation: Avoid preg-
combination with ipilimumab). Treat- nancy; may cause fetal harm. Unknown
ment of classical Hodgkin lymphoma if distributed in breast milk. Females of
(cHL) that relapsed or progressed fol- reproductive potential should use effec-
lowing autologous hematopoietic stem tive contraception during treatment
cell transplant (HSCT) and post-bren- and up to 5 mos after discontinuation.
tuximab, or 3 or more lines of systemic Children: Safety and efficacy not estab-
therapy that includes autologous HSCT. lished. Elderly: May have increased risk
Treatment of recurrent or metastatic of endocrine/hepatic/pulmonary/optic/
squamous cell carcinoma of the head renal injury due to age-related diseases.

Canadian trade name Non-Crushable Drug High Alert drug


838 nivolumab

INTERACTIONS disease progression or unacceptable tox-


DRUG: May enhance adverse/toxic effects icity. (In combination with ipilim-
of belimumab. HERBAL: None signifi- umab): 1 mg/kg, followed by ipilimumab
cant. FOOD: None known. LAB VALUES: on the same day, q3wks for 4 doses. Sub-
Single Therapy: May increase serum sequent single-agent therapy dose is 240
alkaline phosphatase, ALT, AST, potassium. mg q2wks or 480 mg q4wks until disease
May decrease serum sodium. Combo progression or unacceptable toxicity.
Therapy: May increase serum alkaline
Metastatic Non–Small-Cell Lung Cancer
phosphatase, ALT, AST, amylase, creatinine,
(NSCLC)
lipase. May decrease RBC, Hct, Hgb, lym-
IV: ADULTS, ELDERLY: 240 mg q2wks until
phocytes, neutrophils, platelets; serum cal-
disease progression or unacceptable
cium, sodium, magnesium. May increase
toxicity.
or decrease serum calcium, potassium.
Advanced Renal Cell Carcinoma
AVAILABILITY (Rx) (Previously Treated), Urothelial
40 mg/4 mL, 100
Injection Solution: Carcinoma, Hepatocellular Carcinoma,
mg/10 mL, 240 mg/24 mL vials. Melanoma (Adjuvant Treatment)
IV: ADULTS, ELDERLY: 240 mg q2wks or
ADMINISTRATION/HANDLING 480 mg q4wks until disease progression
IV or unacceptable toxicity.
Preparation • Visually inspect solu- cHL (Recurrent or Metastatic)
tion for particulate matter or discolor- IV: ADULTS, ELDERLY: 240 mg once q2wks
N ation. Solution should appear opalescent, or 480 mg once q4wks until disease pro-
colorless to pale yellow. Discard if solu- gression or unacceptable toxicity.
tion is cloudy or contains particulate
matter other than a few translucent to Colorectal Cancer, Metastatic (Single
white proteinaceous particles. • Do not Agent)
shake vial. • Withdraw required dose IV: ADULTS, ELDERLY: 240 mg q2wks or
volume and dilute in 0.9% NaCl or 5% 480 mg once q4wks until disease pro-
Dextrose injection. Final concentration gression or unacceptable toxicity.
will equal 1–10 mg/mL based on volume
of diluent. • Mix by gentle inver- Colorectal Cancer (Metastatic)
sion. • Do not shake. • Discard par- Combination Therapy
tially used or empty vials. IV: ADULTS, ELDERLY: (In combination
Rate of administration • Infuse over with ipilimumab): 3 mg/kg, in com-
60 min using sterile, nonpyrogenic, low bination with ipilimumab, q3wks for 4
protein-binding, 0.2- to 1.2-micron in-line doses. Subsequent single-agent therapy
filter. • Flush IV line upon completion. dose is 240 mg q2wks or 480 mg once
Storage • Refrigerate diluted solution up q4wks until disease progression or unac-
to 24 hrs or store at room temperature for ceptable toxicity.
no more than 4 hrs (includes time of prepa-
ration and infusion). • Do not freeze. Metastatic Small-Cell Lung Cancer (SCLC)
IV: ADULTS, ELDERLY: (Single agent):
IV INCOMPATIBILITIES 3 mg/kg once q2wks until disease pro-
Do not infuse with other medications. gression or unacceptable toxicity. (In
combination with ipilimumab): 1
INDICATIONS/ROUTES/DOSAGE mg/kg once q3wks for 4 combination
Melanoma doses, then 3 mg/kg once q2wks as
(Single Agent):
IV: ADULTS, ELDERLY: single agent until disease progression or
240 mg q2wks or 480 mg q4wks until unacceptable toxicity.

underlined – top prescribed drug


nivolumab 839
RCC (Previously Untreated) Combination other Grade 3 adverse reaction; any life-
Therapy threatening or Grade 4 adverse reaction;
IV: ADULTS, ELDERLY: (In combination requirement for predniSONE 10 mg/day
with ipilimumab): 3 mg/kg, in com- or greater (or equivalent) for more than
bination with ipilimumab, q3wks for 4 12 wks; persistent Grade 2 or 3 adverse
doses. Subsequent single-agent therapy reaction lasting longer than 12 wks.
dose is 240 mg q2wks or 480 mg q4wks
until disease progression or unaccept- Dosage in Renal Impairment
able toxicity. No dose adjustment.
Head and Neck Carcinoma Dosage in Hepatic Impairment
IV: ADULTS, ELDERLY: 240 mg once q2wks Mild to moderate impairment: No
or 480 mg once q4wks until disease pro- dose adjustment. Severe impair-
gression or unacceptable toxicity. ment: Not specified; use caution.

Dose Modification SIDE EFFECTS


Based on Common Terminology Criteria Note: Percentage of side effects may
for Adverse Events (CTCAE). vary depending on the use of single or
Withhold Treatment for Any of the Follow- combination therapy. Frequent (50%–
ing Adverse Events 24%): Fatigue, dyspnea, musculoskeletal
Grade 2 or 3 diarrhea or colitis; single- pain, decreased appetite, cough, nau-
agent therapy–associated colitis; Grade 2 sea, headache, constipation. Occasional
pneumonitis; serum AST or ALT greater (19%–10%): Vomiting, asthenia, diar-
than 3–5 times upper limit of normal rhea, edema, pyrexia, cough, dehydra- N
(ULN) or serum bilirubin 1.5–3 times tion, rash, abdominal pain, chest pain,
ULN; Grade 2 or 3 hypophysitis; Grade 2 arthralgia, decreased weight, blurred
adrenal insufficiency; serum creatinine vision, pruritus, peripheral edema, gen-
greater than 1.5–6 times ULN; Grade 3 eralized pain.
rash; first occurrence of any other Grade
3 adverse reaction. When nivolumab is ADVERSE EFFECTS/TOXIC
administered in combination with ipili- REACTIONS
mumab and nivolumab is withheld, then Anemia, lymphopenia, neutropenia,
ipilimumab should also be withheld. thrombocytopenia is an expected response
Restarting Therapy to therapy. May cause severe immune-
Resume when adverse reactions return to mediated events including interstitial lung
Grade 0 or 1. disease or pneumonitis (3%–10% of pts),
Permanently Discontinue for Any of the colitis (21%–57% of pts), hepatitis (15%–
Following Adverse Events 28% of pts), hypophysitis (13% of pts),
Combo-agent therapy (ipilimumab)– renal failure or nephritis (1%–2% of pts),
associated colitis; Grade 3 or 4 pneu- hyperthyroidism (1% of pts), hypothyroid-
monitis; serum AST or ALT greater than ism (3%–19% of pts), rash (up to 37% of
5 times ULN or serum bilirubin 3 times pts). Other adverse events including auto-
ULN; pts with liver metastasis who begin immune nephropathy, demyelination, dia-
treatment with baseline Grade 2 serum betic ketoacidosis, duodenitis, erythema
ALT or AST elevation who experience multiforme, exfoliative dermatitis, facial
serum ALT or AST elevation greater than and abducens nerve paresis, gastritis, iri-
or equal to 50% from baseline that per- docyclitis, motor dysfunction, pancreatitis,
sists for at least 1 wk; Grade 4 hypophy- psoriasis, sarcoidosis, uveitis, vasculitis,
sitis; Grade 3 or 4 adrenal insufficiency; ventricular arrhythmia, vitiligo reported
serum creatinine greater than 6 times in less than 2% of pts. Severe infusion-
ULN; Grade 4 rash; recurrence of any related reactions reported in less than 1%

Canadian trade name Non-Crushable Drug High Alert drug


840 norepinephrine
of pts. Occurrence of events is dependent matory reactions occur in the following
on use of single or combination therapy. body systems: colon (severe abdominal
Upper respiratory tract infections includ- pain or diarrhea); kidney (decreased or
ing nasopharyngitis, pharyngitis, rhinitis dark-colored urine, flank pain); lung
reported in 11% of pts. Immunogenicity (chest pain, cough, shortness of breath);
(auto-nivolumab antibodies) occurred in liver (bruising easily, dark-colored urine,
8.5% of pts. clay-colored/tarry stools, yellowing of
skin or eyes); pituitary (persistent or
NURSING CONSIDERATIONS unusual headache, dizziness, extreme
BASELINE ASSESSMENT weakness, fainting, vision changes); thy-
roid (trouble sleeping, high blood pres-
Obtain baseline CBC, BMP, ionized cal- sure, fast heart rate [overactive thy-
cium, LFT, TSH; vital signs; urine preg- roid]), (fatigue, goiter, weight gain
nancy. Record weight in kg. Screen for [underactive thyroid]).
history of arrhythmias, pituitary/pulmo-
nary/thyroid disease, autoimmune disor-
ders, diabetes, hepatic/renal impairment;
allergy to predniSONE. Along with routine
norepinephrine
assessment, conduct full dermatologic nor-ep-i-nef-rin
exam, ophthalmologic exam/visual acu- (Levophed)
ity. Receive full medication history and
screen for interactions. j BLACK BOX ALERT jExtrava-
sation may produce severe tissue
INTERVENTION/EVALUATION necrosis, sloughing. Using fine hy-
N podermic needle, liberally infiltrate
Monitor CBC, LFT, serum electrolytes; area with 10–15 mL saline solution
thyroid panel if applicable. Diligently containing 5–10 mg phentolamine.
monitor for immune-mediated adverse Do not confuse Levophed with
events as listed in Adverse Effects/Toxic Levaquin or levoFLOXacin, or
Reactions. Notify physician if any CTCAE norepinephrine with EPINEPH-
toxicities occur (see Appendix M) and rine.
initiate proper treatment. Obtain chest
X-ray if interstitial lung disease, pneu- uCLASSIFICATION
monitis suspected. Screen for tumor lysis PHARMACOTHERAPEUTIC: Alpha,
syndrome in pts with high tumor burden. beta agonist. CLINICAL: Vasopressor.
Monitor I&O, daily weight. If predniSONE
therapy is initiated for immune-mediated
events, monitor capillary blood glucose USES
and screen for corticosteroid side effects. Severe hypotension, treatment of shock
persisting after adequate fluid volume
PATIENT/FAMILY TEACHING replacement.
• Blood levels will be routinely moni-
tored. • Avoid pregnancy; treatment PRECAUTIONS
may cause birth defects or miscarriage. Contraindications: Hypersensitivity to
Do not breastfeed. Females of childbear- norepinephrine. Hypotension related to
ing potential should use effective contra- hypovolemia (except in emergency to
ception during treatment and for at least maintain coronary/cerebral perfusion
5 mos after discontinuation. • Serious until volume replaced), mesenteric/
adverse reactions may affect lungs, GI peripheral vascular thrombosis (unless it
tract, kidneys, or hormonal glands; anti- is lifesaving procedure). Cautions: Con-
inflammatory medication may need to be current use of MAOIs.
started. • Immediately contact physi-
cian if serious or life-threatening inflam-
underlined – top prescribed drug
norepinephrine 841

ACTION IV infusion gradually. Avoid abrupt with-


Stimulates beta1-adrenergic receptors, drawal. • If using peripherally inserted
alpha-adrenergic receptors, increas- catheter, it is imperative to check the IV
ing contractility, heart rate and pro- site frequently for free flow and infused
ducing vasoconstriction. Therapeutic vein for blanching, hardness to vein, cold-
Effect: Increases systemic B/P, coronary ness, pallor to extremity. • If extravasa-
blood flow. tion occurs, area should be infiltrated
with 10–15 mL sterile saline containing
PHARMACOKINETICS 5–10 mg phentolamine (does not alter
Route Onset Peak Duration pressor effects of norepinephrine).
Storage • Do not use if solution is
IV Rapid 1–2 min N/A
brown or contains precipitate. • Store
Localized in sympathetic tissue. Metabo- at room temperature. Diluted solution
lized in liver. Primarily excreted in urine. stable for 24 hrs at room temperature.
LIFESPAN CONSIDERATIONS IV INCOMPATIBILITIES
Pregnancy/Lactation: Readily crosses Pantoprazole (Protonix), regular insulin.
placenta. May produce fetal anoxia due to
uterine contraction, constriction of uter- IV COMPATIBILITIES
ine blood vessels. Children/Elderly: No Amiodarone (Cordarone), calcium glu-
age-related precautions noted. conate, dexmedetomidine (Precedex),
dilTIAZem (Cardizem), DOBUTamine
INTERACTIONS (Dobutrex), DOPamine (Intropin), EPI-
DRUG: MAOIs (e.g., phenelzine, NEPHrine, esmolol (Brevibloc), fentaNYL N
selegiline), antidepressants (tri- (Sublimaze), furosemide (Lasix), halo-
cyclic) may prolong hypertension. peridol (Haldol), heparin, HYDROmor-
SNRIs (e.g., duloxetine), trama- phone (Dilaudid), labetalol (Trandate),
dol may increase tachycardic effect. lipids, LORazepam (Ativan), magnesium,
HERBAL: None significant. FOOD: None midazolam (Versed), milrinone (Prima-
known. LAB VALUES: None significant. cor), morphine, niCARdipine (Cardene),
nitroglycerin, potassium chloride, pro-
AVAILABILITY (Rx) pofol (Diprivan).
Injection Solution: 1 mg/mL.
INDICATIONS/ROUTES/DOSAGE
ADMINISTRATION/HANDLING
b ALERT c If possible, blood, fluid
IV volume depletion should be corrected
Reconstitution • Add 4 mL (4 mg) to before drug is administered.
250 mL D5W (16 mcg/mL). Maximum Acute Hypotension Unresponsive to Fluid
concentration: 32 mL (32 mg) to 250 Volume Replacement
mL (128 mcg/mL). IV infusion: ADULTS, ELDERLY: Initially,
Rate of administration • Closely
administer at 8–12 mcg/min. Adjust
monitor IV infusion flow rate (use infu- rate of flow to desired response. Average
sion pump). • Monitor B/P q2min dur- maintenance range: 2–4 mcg/min (varies
ing IV infusion until desired therapeutic greatly based on clinical situation). CHIL-
response is achieved, then q5min during DREN: Initially, 0.05–0.1 mcg/kg/min;
remaining IV infusion. • Never leave pt titrate to desired effect. Maximum: 2
unattended. • Maintain B/P at 90–100 mcg/kg/min.
mm Hg in previously normotensive pts,
and 30–40 mm Hg below preexisting B/P Dosage in Renal/Hepatic Impairment
in previously hypertensive pts. • Reduce No dose adjustment.

Canadian trade name Non-Crushable Drug High Alert drug


842 nortriptyline

SIDE EFFECTS Do not confuse Aventyl with


Norepinephrine produces less pro- Bentyl, or nortriptyline with
nounced, less frequent side effects than amitriptyline, desipramine, or
EPINEPHrine. Occasional (5%–3%): Anx- Norpramin.
iety, bradycardia, palpitations. Rare (2%– uCLASSIFICATION
1%): Nausea, anginal pain, shortness of
breath, fever. PHARMACOTHERAPEUTIC: Tricyclic
compound. CLINICAL: Antidepressant.
ADVERSE EFFECTS/TOXIC
REACTIONS
USES
Extravasation may produce tissue necro-
sis, sloughing. Overdose manifested Treatment of symptoms of unipolar major
as severe hypertension with violent depression. OFF-LABEL: Adjunctive ther-
headache (may be first clinical sign of apy for smoking cessation, myofascial
overdose), arrhythmias, photophobia, pain, postherpetic pain, orofacial pain,
retrosternal or pharyngeal pain, pallor, chronic pain, irritable bowel syndrome.
diaphoresis, vomiting. Prolonged therapy PRECAUTIONS
may result in plasma volume depletion.
Hypotension may recur if plasma volume Contraindications: Hypersensitivity to nor­
is not maintained. triptyline. Use during acute recovery pe-
riod after MI. Use of MAOI intended to
treat psychiatric disorders (concurrently
NURSING CONSIDERATIONS or within 14 days of discontinuing ei-
N BASELINE ASSESSMENT ther nortriptyline or MAOI). Initiation of
Assess ECG, B/P continuously (be alert nortriptyline in pt receiving linezolid or
to precipitous B/P drop). Be alert to pt methylene blue. Cautions: Prostatic hy-
complaint of headache. perplasia, history of urinary retention/ob-
struction, narrow-angle glaucoma, diabe-
INTERVENTION/EVALUATION tes, history of seizures, hyperthyroidism,
Monitor IV flow rate diligently. Assess for cardiac/hepatic/renal disease, psychosis,
extravasation characterized by blanching increased intraocular pressure, pts at high
of skin over vein, coolness (results from risk for suicide, elderly pts.
local vasoconstriction); color, tempera-
ture of IV site extremity (pallor, cyanosis, ACTION
mottling). Assess nailbed capillary refill. Blocks reuptake of neurotransmitters
Monitor I&O; measure output hourly, (norepinephrine, serotonin) at neuronal
report urine output less than 30 mL/hr. presynaptic membranes, increasing their
Once B/P parameter has been reached, availability at postsynaptic receptor sites.
IV infusion should not be restarted unless Therapeutic Effect: Relieves depres-
systolic B/P falls below 90 mm Hg. sion, anxiety disorders, nocturnal enuresis.
PHARMACOKINETICS
nortriptyline Rapidly absorbed. Widely distributed.
Extensively bound to plasma proteins.
nor-trip-ti-leen Metabolized in liver. Excreted primarily
(Aventyl , Norventyl , Pamelor) in urine. Half-life: Adults: 14–51 hrs.
j BLACK BOX ALERT jIncreased Elderly: 23–79 hrs.
risk of suicidal thinking and behavior
in children, adolescents, young adults LIFESPAN CONSIDERATIONS
18–24 yrs with major depressive Pregnancy/Lactation: Crosses placenta,
disorder, other psychiatric disorders. excreted in breast milk. Children: Safety

underlined – top prescribed drug


nortriptyline 843
and efficacy not established in children Depression
younger than 6 yrs. Elderly: Use caution. PO: ADULTS: Initially, 25 mg once daily.
May increase to usual dose of 25 mg 3–4
INTERACTIONS times/day up to 150 mg/day. Total daily
DRUG: Aclidinium, ipratropium, dose may be given as a single dose. Adjust
tiotropium, umeclidinium may dose based on response and tolerability.
increase anticholinergic effect. CNS ELDERLY: Initially, 30–50 mg at bedtime.
depressants (e.g., alcohol, mor- May increase by 25 mg every 3–7 days.
phine, oxycodone, zolpidem) may Maximum: 150 mg/day.
increase CNS depression. May increase
arrhythmogenic effect of dronedar- Enuresis
one. May increase adverse effects of PO: CHILDREN 6 YRS AND OLDER: Ini-
escitalo-pram. Cimetidine may tially, 10–20 mg/day. May titrate up to
increase concentration, risk of toxicity. maximum daily dose of 40 mg/day.
MAOIs (e.g., phenelzine, selegiline) Dosage in Renal Impairment
may increase risk of neuroleptic malig- No dose adjustment.
nant syndrome, seizures, hyperpyrexia,
hypertensive crisis. HERBAL: St. Johns Dosage in Hepatic Impairment
wort may decrease concentration/ Use caution.
effect. Herbals with sedative prop-
erties (e.g., chamomile, kava kava, SIDE EFFECTS
valerian) may increase CNS depres- Frequent: Drowsiness, fatigue, dry mouth,
sion. FOOD: Grape juice, carbonated blurred vision, constipation, delayed mic-
beverages may decrease effectiveness. turition, orthostatic hypotension, diapho- N
Grapefruit products may increase risk resis, impaired concentration, increased
of side effects. LAB VALUES: May alter appetite, urinary retention. Occasional: GI
serum glucose, ECG readings. Thera- disturbances (nausea, GI distress, metallic
peutic peak serum level: 6–10 mcg/ taste), photosensitivity. Rare: Paradoxical
mL; therapeutic trough serum level: reactions (agitation, restlessness, night-
0.5–2 mcg/mL. Toxic peak serum mares, insomnia), extrapyramidal symp-
level: greater than 12 mcg/mL; toxic toms (particularly fine hand tremor).
trough serum level: greater than 2
mcg/mL.
ADVERSE EFFECTS/TOXIC
AVAILABILITY (Rx) REACTIONS
Capsules: 10 mg, 25 mg, 50 mg, 75 mg. High dosage may produce cardiovascu-
Oral Solution: 10 mg/5 mL. lar effects (severe orthostatic hypoten-
sion, dizziness, tachycardia, palpitations,
ADMINISTRATION/HANDLING arrhythmias), altered temperature regu-
PO lation (hyperpyrexia, hypothermia).
• Give with food, milk if GI distress Abrupt discontinuation from prolonged
occurs. • Dilute oral solution in water, therapy may produce headache, malaise,
milk, or fruit juice. Give immediately. nausea, vomiting, vivid dreams.
(Do not mix with grape juice/carbonated
beverages.) NURSING CONSIDERATIONS
BASELINE ASSESSMENT
INDICATIONS/ROUTES/DOSAGE
Assess for suicidal ideation/tendencies,
b ALERT c At least 14 days must elapse behavior, thought content, appearance.
between use of MAOIs and nortripty- Obtain baseline glucose, cholesterol
line. When discontinuing, gradually taper levels. For pts on long-term therapy,
dose to minimize withdrawal symptoms.

Canadian trade name Non-Crushable Drug High Alert drug


844 nortriptyline
hepatic/renal function tests, blood counts PATIENT/FAMILY TEACHING
should be performed periodically. • Slowly go from lying to standing to
INTERVENTION/EVALUATION
avoid hypotensive effect; tolerance to
postural hypotension, sedative, anticho-
Supervise suicidal-risk pt closely during linergic effects usually develops during
early therapy (as depression lessens, en- early therapy. • Avoid alcohol. • Avoid
ergy level improves, increasing suicide tasks that require alertness, motor skills
potential). Assess appearance, behavior, until response to drug is estab-
speech pattern, level of interest, mood. lished. • Therapeutic effect may be
Monitor daily pattern of bowel activity, noted in 2 wks or longer. • Photosensi-
stool consistency. Avoid constipation with tivity to sun may occur; use sunscreen,
increased fluids, bulky foods. Monitor protective clothing. • Dry mouth may
B/P, pulse for hypotension, arrhythmias, be relieved by sugarless gum, sips of
weight. Assess for urinary retention. water. • Report visual disturbances,
Therapeutic peak serum level: 6–10 worsening depression, suicidal ideation,
mcg/mL; trough serum level: 0.5–2 mcg/ unusual changes in behavior (esp. at
mL. Toxic peak serum level: greater than initiation of therapy or with changes in
12 mcg/mL; toxic trough: greater than 2 dosage). • Do not abruptly discontinue
mcg/mL. medication.

underlined – top prescribed drug


obinutuzumab 845
PHARMACOKINETICS
obinutuzumab Metabolism and elimination not speci-
fied. Half-life: 28 days.
oh-bi-nue-tooz-ue-mab
(Gazyva) LIFESPAN CONSIDERATIONS
j BLACK BOX ALERT jHepatitis Pregnancy/Lactation: Unknown if
B virus reactivation, resulting in distributed in breast milk. Monoclonal
hepatic failure, fulminant hepatitis,
and death have occurred. Screen antibodies are known to cross placenta.
all pts for hepatitis B virus infection Effective contraception, discontinuation
before initiating treatment. Progres- of breastfeeding recommended during
sive multifocal leukoencepha- therapy and for at least 18 mos after dis-
lopathy (PML) including fatal PML continuation. Children: Safety and effi-
reported.
cacy not established. Elderly: May have
uCLASSIFICATION increased risk of adverse reactions.
PHARMACOTHERAPEUTIC: Anti- INTERACTIONS
CD20 monoclonal antibody. CLINI-
CAL: Antineoplastic.
DRUG: May increase hypotensive effect of
ACE inhibitors (e.g., enalapril, lisin-
opril), angiotensin receptor block-
ers (e.g., losartan), beta blockers
USES (e.g., metoprolol). May decrease the
Treatment of previously untreated therapeutic effect of BCG (intravesical),
chronic lymphocytic leukemia (CLL), in vaccines (live). May increase adverse
combination with chlorambucil. Treat- effects of belimumab, natalizumab,
ment of follicular lymphoma (in combi- vaccines (live). HERBAL: Echinacea
nation with bendamustine) in pts who may diminish the therapeutic effect. O
relapsed after, or are refractory to, a FOOD: None known. LAB VALUES: May
riTUXimab-containing regimen. Treat- increase serum alkaline phosphatase, ALT,
ment of previously untreated stage II AST, bilirubin, creatinine, uric acid. May
bulky, stage III, or stage IV follicular decrease albumin, Hgb, Hct, lymphocytes,
lymphoma in combination with chemo- neutrophils, platelets; serum potassium,
therapy and followed by obinutuzumab sodium.
monotherapy.
AVAILABILITY (Rx)
PRECAUTIONS 1,000 mg/40 mL (25
Injection Solution:
Contraindications: Hypersensitivity to mg/mL) single-use vial.
obinutuzumab. Cautions: Pts showing
evidence of prior HBV infection, preexist- ADMINISTRATION/HANDLING
ing cardiac/pulmonary impairment; b ALERT c Administer via dedicated
hematologic abnormalities (e.g., leuko- line. Do not administer IV push or bolus.
penia, thrombocytopenia); electrolyte Withhold hypertensive medications at
imbalance; avoid with active infection. least 12 hrs before and 1 hr after admin-
istration. Do not mix with dextrose-con-
ACTION taining fluids.
Targets CD20 antigen expressed on sur-
IV
face of B lymphocytes. Mediates B-cell
lysis by activating complement-dependent Reconstitution • Visually inspect for
cytotoxicity, antibody-dependent cellular particulate matter or discoloration. • For
cytotoxicity. Therapeutic Effect: Inhib- 100-mg dose: withdraw 40 mL solution
its tumor cell growth and proliferation in from vial and dilute only 4 mL (100 mg) in
chronic lymphocytic leukemia. 100 mL 0.9% NaCl for immediate
Canadian trade name Non-Crushable Drug High Alert drug
846 obinutuzumab
administration. Dilute remaining 36 mL obinutuzumab (as monotherapy) 1,000
(900 mg) into 250 mL 0.9% NaCl at same mg q2mos for 2 yrs.
time and refrigerate for up to 24 hrs for
cycle 1: day 2. For remaining infusions Follicular Lymphoma (previously
(day 8 and day 15 of cycle 1 and day 1 of untreated)
cycles 2–6), dilute 40 mL (1,000 mg) IV: ADULTS, ELDERLY: Cycle 1 (either
solution in 250 mL NaCl infusion in combination with bendamustine
bag. • Gently mix by inversion. • Do or with CHOP or CVP chemother-
not shake. apy): 1,000 mg wkly on days 1, 8, and
Rate of administration • Day 1 of 15. Cycles 2–6 (in combination with
cycle 1 (100 mg): Infuse over 4 hrs (25 bendamustine): 1,000 mg on day 1
mg/hr). • Do not increase infusion q28days for 5 doses. Cycles 2–8 (in
rate. • Day 2 of cycle 1 (900 mg): combination with CHOP): 1,000 mg
Infuse at 50 mg/hr. • May increase by on day1 q21days for 5 doses (with CHOP),
50 mg/hr every 30 min to maximum rate then 1,000 mg on day 1 q21 days for 2
of 400 mg/hr. • Increase rate based on doses (as monotherapy). Cycles 2–8
tolerability. (in combination with CVP): 1,000
Storage • Solution should appear mg on day1 q21days for 7 doses. Then
clear, colorless to slightly brown. • May as monotherapy: 1,000 mg q2mos for
refrigerate diluted solution up to 24 hrs. up to 2 yrs beginning approximately 2 mos
after last induction phase.
INDICATIONS/ROUTES/DOSAGE
Dosage in Renal/Hepatic Impairment
Chronic Lymphocytic Leukemia (CLL) No dose adjustment.
b ALERT c Premedicate with glucocor-
ticoid, acetaminophen, and antihistamine SIDE EFFECTS
O
to decrease severity of infusion reaction. Frequent (69%): Infusion reactions (pru-
Consider premedication with antihyper- ritus, flushing, urticaria). Occasional
uricemics (allopurinol) 12–24 hrs for (10%): Pyrexia, cough.
pts with high tumor burden or high cir-
culating absolute lymphocyte count ADVERSE EFFECTS/TOXIC
greater than 25 × 109/L. Recommend REACTIONS
antimicrobial prophylaxis throughout Thrombocytopenia, neutropenia, leukope-
treatment for pts with neutropenia. nia, lymphopenia (47%–80% of pts) are
IV: ADULTS/ELDERLY: Six treatment cyc­les expected responses to therapy, but more
of 28-day cycle. Day 1 of cycle 1: 100 severe reactions including bone marrow
mg. Day 2 of cycle 1: 900 mg. Day failure, febrile neutropenia, opportunis-
8 and Day 15 of cycle 1: 1000 mg. tic infection may result in life-threatening
Cycles 2–6: 1000 mg on day 1 of each events. Hepatitis B virus reactivation may
subsequent 28-day cycle for 5 doses. occur. Infusion reactions including hypo-
Discontinue treatment if any severe to life- tension, tachycardia, dyspnea, broncho-
threatening infusion reactions occur. spasm, wheezing, laryngeal edema, nausea,
vomiting, flushing, pyrexia may occur dur-
Follicular Lymphoma (Relapsed/ ing infusion. Tumor lysis syndrome may
Refractory) present as acute renal failure, hypocalce-
IV: ADULTS, ELDERLY: Six treatment mia, hyperuricemia, hyperphosphatemia
cycles of 28 days (in combination with within 12–24 hrs of infusion. Immunoge-
bendamustine). Cycle 1: 1,000 mg on nicity (autoantibodies) occurred in 13% of
days 1, 8, 15. Cycles 2–6: 1,000 mg on pts. Progressive multifocal leukoencepha-
day 1 of each subsequent 28-day cycle lopathy (PML) occurred rarely and may
for 5 doses. If achieves stable disease, include weakness, paralysis, vision loss,
complete or partial response, continue aphasia, cognition impairment.
underlined – top prescribed drug
ocrelizumab 847

NURSING CONSIDERATIONS uCLASSIFICATION


PHARMACOTHERAPEUTIC: Anti-
BASELINE ASSESSMENT CD20 monoclonal antibody. CLINI-
Obtain baseline CBC, BMP, ionized cal- CAL: Multiple sclerosis agent.
cium, phosphate, uric acid; vital signs.
Screen for history of anemia, asthma,
­arrhythmias, COPD, diabetes, GI bleed- USES
ing, hypertension, hepatitis B virus Treatment of adult pts with relapsing or
­infection, hepatic/renal impairment, pe- primary progressive forms of multiple
ripheral edema. Receive full medication sclerosis (MS).
history, esp. hypertension, anticoagulant
medications. Perform baseline visual PRECAUTIONS
acuity. Offer emotional support. Contraindications: Life-threatening infu-
INTERVENTION/EVALUATION
sion reaction to ocrelizumab. Active hep-
atitis B virus (HBV) infection confirmed
Monitor CBC, serum electrolytes, LFT, by positive results for hepatitis B surface
vital signs. Monitor all pts for cardiovas- antigen (HBsAg) and anti-HBV tests.
cular alterations, respiratory distress. If Cautions: History of chronic opportu-
respiratory reactions occur, consider nistic infections (esp. bacterial, invasive
administration of oxygen, EPINEPHrine, fungal, mycobacterial, protozoal, viral,
albuterol treatments. Locate rapid- tuberculosis); active infection, condi-
sequence intubation kit if respiratory tions predisposing to infection (e.g.,
compromise occurs. Monitor strict I&O, diabetes, immunocompromised pts,
hydration status. If PML suspected, con- renal failure, open wounds); intolerance
sult neurologist for proper management. to corticosteroids; history of depres-
Obtain ECG for palpitations, severe hypo- sion, malignancies, breast cancer. Avoid O
kalemia, hyponatremia. administration of live or live attenuated
PATIENT/FAMILY TEACHING vaccines during treatment and after dis-
• Avoid pregnancy. • Report any yel- continuation until B-cells are no longer
lowing of skin or eyes, abdominal pain, depleted.
bruising, black/tarry stools, amber or ACTION
bloody urine. • Fever, cough, burning
with urination, body aches, chills may in- Monoclonal antibody that is directed
dicate acute infection. • Avoid use of live against B cells, which express the cell
virus vaccines. • Avoid alcohol. • Im- surface antigen CD20 (thought to influ-
mediately report difficult breathing, severe ence the course of MS through antigen
coughing, chest tightness, wheez- presentation, autoantibody produc-
ing. • Paralysis, vision changes, im- tion, cytokine regulation, and forma-
paired speech, altered mental status may tion of ectopic lymphoid aggregates in
indicate life-threatening neurologic event. meninges). Binds to the cell surface
to deplete CD20-expressing B cells.
Therapeutic Effect: Reduces pro-
gression of MS.
ocrelizumab
PHARMACOKINETICS
ok-re-liz-ue-mab Onset of action: serum CD-19+
(Ocrevus) B-cell count reduced within 14 days.
Do not confuse ocrelizumab Duration of action: 72 wks (Range:
with certolizumab, daclizumab, 27–175 wks). Antibodies are primar-
efalizumab, mepolizumab, ily cleared by catabolism. Half-life:
natalizumab, or omalizumab. 26 days.
Canadian trade name Non-Crushable Drug High Alert drug
848 ocrelizumab

LIFESPAN CONSIDERATIONS in-line filter. If tolerated, increase rate by


Pregnancy/Lactation: May cause 30 mL/hr q30min to a maximum rate of
transient peripheral B-cell depletion and 180 mL/hr for a duration of 2.5 hrs or
lymphocytopenia in neonates when used longer. • Subsequent Infusions:
during pregnancy. Immunoglobulins are Start at 40 mL/hr via dedicated line using
known to cross the placenta. Females of 0.2- or 0.22-micron in-line filter. If toler-
reproductive potential must use effective ated, increase rate by 40 mL/hr q30min
contraception during treatment and up to a maximum rate of 200 mL/hr for a
to 6 mos after discontinuation. Unknown duration of 3.5 hrs or longer. • Mild
if distributed in breast milk; however, Infusion Reactions: Decrease rate by
immunoglobulin G (IgG) is present in 50% and continue reduced rate for at
breast milk. Breastfeeding not recom- least 30 min. If tolerated, may increase
mended. Children: Safety and efficacy infusion rate as described
not established. Elderly: No age-related above. • Severe Infusion Reactions:
precautions noted. Interrupt infusion until symptoms
resolve, then resume infusion at 50% of
INTERACTIONS the initial infusion rate. • Life-threat-
DRUG: May decrease effect of BCG, ening Infusion Reaction: Immediately
vaccines (live). May increase adverse stop infusion and permanently discon-
effects/toxicity of belimumab, natali- tinue; do not restart.
Storage • May refrigerate diluted
zumab, tacrolimus. HERBAL: Echi-
nacea may diminish therapeutic effect. solution up to 24 hrs or store at room
FOOD: None known. LAB VALUES: May
temperature for up to 8 hrs (includes
decrease immunoglobulin A (IgA), infusion time). • If diluted solution is
immunoglobulin M (IgM), immunoglob- refrigerated, allow to warm to room tem-
O ulin G (IgG), neutrophils. perature before administration. • Dis-
card solution if not administered within
AVAILABILITY (Rx) required time frame.
Injection Solution: 300 mg/10 mL (30 IV INCOMPATIBILITIES
mg/mL).
Do not dilute with other IV solutions. Do
ADMINISTRATION/HANDLING not mix or infuse with other medi­
cations.
IV
Preparation • Visually inspect for INDICATIONS/ROUTES/DOSAGE
particulate matter or discoloration. Solu- b ALERT c Must be administered under
tion should appear clear to slightly opal- the direct supervision of health care pro-
escent, colorless to pale brown in fessionals with access to emergency
color. • Do not use if solution is cloudy, medical supplies and who are trained to
discolored, or if visible particles are manage severe infusion reactions. If a
observed. • Withdraw proper dose dose is missed, administer as soon as
from vial (10 mL for 300-mg dose; 20 mL possible; do not wait until the next regu-
for 600-mg dose) and dilute into 0.9% larly scheduled dose. Reset administra-
NaCl bag to a final concentration of tion schedule so that the next subsequent
approx. 1.2 mg/mL (300-mg dose in 250 infusion is 6 mos after the most recent
mL 0.9% NaCl; 600-mg dose in 500 mL dose. Subsequent doses must be sepa-
0.9% NaCl). • Mix by gentle inver- rated by at least 5 mos.
sion. • Do not shake or agitate. Premedication
Rate of administration • First and • To reduce severity and frequency
Second Infusion: Start at 30 mL/hr via of infusion reaction, premedicate
dedicated line using 0.2- or 0.22-micron with methylprednisolone 100 mg (or
underlined – top prescribed drug
ocrelizumab 849
equivalent) approx. 30 min prior to infu- increase risk of malignancies including
sion and an antihistamine (e.g., diphen- breast cancer. Immunogenicity (auto
hydramine) approx. 30–60 min prior to anti-ocrelizumab antibodies) reported
infusion. • Consider an antipyretic in 1% of pts. Depression reported in 8%
(e.g., acetaminophen) based on previous of pts.
infusion reactions.
NURSING CONSIDERATIONS
Multiple Sclerosis
IV: ADULTS, ELDERLY: 300 mg once at wk BASELINE ASSESSMENT
0 and wk 2, then 600 mg q6mos (begin- Assess baseline symptoms of MS (e.g.,
ning 6 mos after the first 300-mg dose). bladder/bowel dysfunction, cognitive im-
Observe pt for at least 1 hr after comple- pairment, depression, dysphagia, fatigue,
tion of infusion. gait disorder, numbness/tingling, pain,
seizures, spasticity, tremors, weakness).
Dosage in Renal/Hepatic Impairment
Obtain vital signs. Question history of hy-
Mild impairment: No dose adjust-
persensitivity reactions, infusion-related
ment. Moderate to severe impair- reactions. Ensure that proper resuscitative
ment: Not specified; use caution.
equipment, medical supplies are readily
SIDE EFFECTS available (e.g., albuterol, antipyretics, anti-
histamines, epinephrine, isotonic IV fluids,
Occasional (8%–5%): Back pain, cough, bag-valve mask, oxygen, rapid sequence in-
diarrhea, peripheral edema, extremity tubation kit). Screen all pts for active HBV.
pain. Pts who test negative for HBsAg and posi-
ADVERSE EFFECTS/TOXIC tive for anti-HBcAb+ should be referred to
REACTIONS a hepatic specialist. If applicable, immuni-
zations should be up-to-date according to O
Infusion-related reactions including guidelines at least 6 wks prior to initiation.
bronchospasm, dizziness, dyspnea, ery- Question history of chronic infections, her-
thema, fatigue, flushing, headache, hypo- pes infection, depression, m ­ alignancies,
tension, nausea, oropharyngeal pain, breast cancer. Screen for active infection.
pharyngeal/laryngeal edema, pruritus, Verify use of effective contraception in fe-
pyrexia, rash, tachycardia, throat irrita- males of reproductive potential.
tion, urticaria was reported in 34%–40%
of pts. Serious infusion reactions requir- INTERVENTION/EVALUATION
ing hospitalization occurred in less than Monitor vital signs. Diligently monitor for
1% of pts. Infections including upper infusion-related reactions during infusion
respiratory tract infections (40%–49% and for at least 1 hr after completion (esp.
of pts), lower respiratory tract infections during initial infusions). If severe or life-
(10% of pts), skin infections (16% of threatening reactions occur, immediately
pts), herpes infection (6% of pts) may stop infusion and provide appropriate
occur. Progressive multifocal leukoen- medical support. Due to risk of respira-
cephalopathy (PML), an opportunistic tory compromise, pts with bronchospasm,
viral infection of the brain caused by the dyspnea, hypoxia should be given imme-
JC virus, has occurred in pts treated with diate supplemental oxygen, hypersensitiv-
other anti-CD20 antibodies; may result ity medications, hemodynamic support. If
in progressive permanent disability and laryngeal or pharyngeal edema occurs,
death. Symptoms of PML include altered airway protection or possible intubation
mental status, aphasia, paralysis, vision may be required. Mild to moderate infu-
loss, weakness. HBV reactivation was sion reactions may require interruption of
reported in pts treated with other anti- infusion, decrease of infusion rate, symp-
CD20 antibodies; may result in fulminant tom management. Closely monitor for
hepatitis, hepatic failure, death. May
Canadian trade name Non-Crushable Drug High Alert drug
850 octreotide
HBV reactivation, symptoms of PML, new uCLASSIFICATION
malignancies including breast cancer, in- PHARMACOTHERAPEUTIC: Somato-
fections. Conduct neurologic assessment. statin analogue. CLINICAL: Secretory
Assess for symptom improvement of MS. inhibitory, growth hormone suppres-
sant; antidiarrheal.
PATIENT/FAMILY TEACHING
• Life-threatening infusion reactions, al-
lergic reactions may occur during infusion USES
and up to 24 hrs after completion of Control of diarrhea and flushing in pts
infusion. Immediately report difficulty
­ with metastatic carcinoid tumors, treat-
breathing, chest pain, chest tightness, ment of watery diarrhea associated with
chills, dizziness, fast heart rate, fever, vasoactive intestinal peptic-secreting
flushing, headache, hives, itching, low tumors (VIPomas), acromegaly (to
blood pressure, nausea, throat pain or reduce blood levels of growth hormone
swelling, rash. • If applicable, vaccina- and insulin-like growth factor). OFF-
tions should be up-to-date at least 6 wks LABEL: Control of bleeding esophageal
before starting treatment. Do not receive varices, treatment of AIDS-associated
live vaccines. • Treatment may depress secretory diarrhea, diarrhea, diarrhea
your immune system and reduce your associated with graft-vs-host disease,
ability to fight infection. Report symptoms chemotherapy-induced diarrhea, insu-
of infection such as body aches, burning linomas, small-bowel fistulas, Zollinger-
with urination, chills, cough, fatigue, fever. Ellison syndrome, Cushing’s syndrome,
Avoid those with active infection. • Avoid hypothalamic obesity, malignant bowel
pregnancy. Females of childbearing poten- obstruction, postgastrectomy dumping
tial should use effective contraception dur- syndrome, islet cell tumors, sulfonylurea-
O ing treatment and for at least 6 mos after induced hypoglycemia.
last dose. Do not breastfeed. • Due to
pretreatment with a corticosteroid, pts PRECAUTIONS
with diabetes may experience a transient Contraindications: Hypersensitivity to
rise in blood sugar levels. • PML, an op- octreotide. Cautions: Diabetic pts with
portunistic viral infection of the brain, may gastroparesis, renal failure, hepatic
cause progressive, permanent disabilities impairment, HF, concomitant medica-
and death. Report symptoms of PML such tions altering heart rate or rhythm. Con-
as confusion, memory loss, paralysis, current use of medications that prolong
trouble speaking, vision loss, seizures,
­ QT interval, elderly pts.
weakness. • Treatment may cause reac-
tivation of HBV, depression, new cancers ACTION
including breast cancer. • Notify physi- Suppresses secretion of serotonin, gastrin,
cian if symptoms of MS do not improve. VIP, insulin, glucagon, secretin, pancreatic
polypeptide. Therapeutic Effect: Pro-
longs intestinal transit time. Decreases
octreotide growth hormone in acromegaly.

ock-tree-oh-tide PHARMACOKINETICS
(SandoSTATIN, SandoSTATIN LAR Route Onset Peak Duration
Depot) SQ N/A N/A Up to 12 hrs
Do not confuse SandoSTATIN
with SandIMMUNE, SandoSTA- Rapidly, completely absorbed from injec-
TIN LAR, sargramostim, or tion site. Protein binding: 65%. Metabo-
simvastatin. lized in liver. Excreted in urine. Removed
by hemodialysis. Half-life: 1.7–1.9 hrs.
underlined – top prescribed drug
octreotide 851

LIFESPAN CONSIDERATIONS INDICATIONS/ROUTES/DOSAGE


Pregnancy/Lactation: Unknown if dis- Note: Schedule injections between
tributed in breast milk. Children: Safety meals (to decrease GI effects).
and efficacy not established. Elderly: No
age-related precautions noted. Carcinoid Tumor
IV, SQ: (Sandostatin): ADULTS, ELDERLY:
INTERACTIONS Initial 2 wks, 100–600 mcg/day in 2–4
DRUG: May decrease effectiveness of divided doses. Range: 50–750 mcg.
cycloSPORINE. Glucagon, growth IM: (Sandostatin Lar): ADULTS,
hormone, insulin, oral antidiabet- ELDERLY: Must be stabilized on SQ octreo-
ics (e.g., glipiZIDE, metFORMIN) tide for at least 2 wks. 20 mg q4wks for 2
may alter glucose concentrations. mos, then modify based on response.
HERBAL: Herbals with hypoglyce-
Vasoactive Intestinal Peptic-Secreting
mic properties (e.g., fenugreek) may Tumor (VIPoma)
increase hypoglycemic effect. FOOD: None IV, SQ: (Sandostatin): ADULTS, ELDERLY:
known. LAB VALUES: May decrease serum Initial 2 wks, 200–300 mcg/day in 2–4
thyroxine (T4). May increase serum alka- divided doses. Titrate dose based on
line phosphatase, ALT, AST, GGT. response/tolerance. Range: 150–750 mcg.
AVAILABILITY (Rx) IM: (Sandostatin Lar): ADULTS, ELDERLY:
Must be stabilized on SQ octreotide for at
Injection Solution: (SandoSTATIN): 50
least 2 wks; 20 mg q4wks for 2 mos, then
mcg/mL, 100 mcg/mL, 200 mcg/mL, 500 modify based on response.
mcg/mL, 1,000 mcg/mL. Injection Suspen-
sion: (SandoSTATIN LAR): 10-mg, 20-mg, Acromegaly
30-mg vials. IV, SQ: (Sandostatin): ADULTS, ELDERLY: O
Initially, 50 mcg 3 times/day. Increase
ADMINISTRATION/HANDLING as needed. Range: 300–1,500 mcg/day.
b ALERT c SandoSTATIN may be given Usual effective dose: 100 mcg 3 times/
IV, IM, SQ. SandoSTATIN LAR Depot may day.
be given only IM. Refrigerate. IM: (Sandostatin Lar): ADULTS, ELDERLY:
Must be stabilized on SQ octreotide for
IM
at least 2 wks. 20 mg q4wks for 3 mos,
• Give immediately after mixing. • then modify based on response. Maxi-
Administer deep IM in large muscle mass mum: 40 mg q4wks.
at 4-wk intervals. • Avoid deltoid
injections. Dosage in Renal/Hepatic Impairment
No dose adjustment.
SQ
• Do not use if discolored or particu- SIDE EFFECTS
lates form. • Avoid multiple injections Frequent (10%–6%; 58%–30% in Acromeg-
at same site within short periods. aly Pts): Diarrhea, nausea, abdominal
IV discomfort, headache, injection site pain.
Occasional (5%–1%): Vomiting, flatulence,
• Dilute in 50–100 mL 0.9% NaCl or D5W
and infuse over 15–30 min. In emergency, constipation, alopecia, facial flushing,
may give IV push over 3 min. Following pruritus, dizziness, fatigue, arrhythmias,
dilution, stable for 96 hrs at room tem- ecchymosis, blurred vision. Rare (less than
1%): Depression, diminished libido, ver-
perature when diluted with 0.9% NaCl (24
hrs with D5W). Infuse over 15–30 min. tigo, palpitations, dyspnea.

Canadian trade name Non-Crushable Drug High Alert drug


852 ofatumumab

ADVERSE EFFECTS/TOXIC therapy. Treatment of CLL refractory to


REACTIONS fludarabine and alemtuzumab.
Increased risk of cholelithiasis. Pro-
PRECAUTIONS
longed high-dose therapy may produce
hypothyroidism. GI bleeding, hepatitis, Contraindications: Hypersensitivity to
seizures occur rarely. ofatumumab. Cautions: Carriers of hepa-
titis B virus.
NURSING CONSIDERATIONS
ACTION
BASELINE ASSESSMENT Binds to CD20 molecule, the antigen on
Establish baseline B/P, weight, thyroid surface of B-cell lymphocytes; inhib-
function, serum glucose, electrolytes. its early-stage B-lymphocyte activation.
INTERVENTION/EVALUATION
Therapeutic Effect: Controls tumor
growth, triggers cell death.
Monitor serum glucose, electrolytes,
thyroid function. In acromegaly, monitor PHARMACOKINETICS
growth hormone levels. Weigh every 2–3 Eliminated through both a target-inde-
days, report over 5-lb gain per wk. Moni- pendent route and a B-cell–mediated
tor B/P, pulse, respirations periodically route. Due to depletion of B cells, clear-
during treatment. Be alert for decreased ance is decreased substantially after sub-
urinary output, peripheral edema. Moni- sequent infusions compared with first
tor daily pattern of bowel activity, stool infusion. Half-life: 12–16 days.
consistency.
PATIENT/FAMILY TEACHING
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if dis-
• Therapy should provide significant
O improvement of severe, watery diarrhea. tributed in breast milk. Children: Safety
and efficacy not established. Elderly: No
age-related precautions noted.
ofatumumab INTERACTIONS
DRUG: Bone marrow depressants
oh-fa-tue-mue-mab (e.g., cladribine) may increase myelo-
(Arzerra) suppression. Live virus vaccines may
j BLACK BOX ALERT jHepatitis potentiate virus replication, increase vac-
B virus (HBV) reactivation may cine side effects, decrease pt’s antibody
occur, resulting in hepatitis, hepatic
failure, death. Progressive multifo- response to vaccine. HERBAL: Echi-
cal leukoencephalopathy (PML) nacea may decrease concentration/
resulting in death may occur. effects. FOOD: None known. LAB
Do not confuse ofatumumab VALUES: May decrease neutrophils,
with omalizumab. platelets.
uCLASSIFICATION AVAILABILITY (Rx)
PHARMACOTHERAPEUTIC: Anti- Injection Solution: 100 mg/5 mL, 1000
CD20 monoclonal antibody. CLINI- mg/50 mL.
CAL: Antineoplastic.
ADMINISTRATION/HANDLING
IV
USES
Treatment of chronic lymphocytic leu- b ALERT c Do not give by IV push or
kemia (CLL) in pts previously untreated, bolus. Use in-line filter supplied with
relapsed, or who require extended product.

underlined – top prescribed drug


ofatumumab 853
Reconstitution • 300-mg dose: i­nfusion reaction of any severity occurs
Withdraw and discard 15 mL from 1,000 (do not resume for Grade 4 reaction).
mL 0.9% NaCl bag. • Withdraw 5 mL
from each of 3 single-use 100-mg vials Chronic Lymphocytic Leukemia
and add to bag. • Gently invert. (Untreated)
• 1,000-mg dose: Withdraw and dis- IV infusion: ADULTS, ELDERLY: Cycle 1:
card 50 mL from 1,000 mL NaCl bag. 300 mg, then 1,000 mg on day 8. Subse-
Withdraw 50 mL from 1 single-use quent cycles: 1,000 mg on day 1 q28days.
1,000-mg vial and add to bag. • Gently Continue for at least 3 cycles or a maxi-
invert to mix. 2,000-mg dose: With- mum of 12 cycles (in combination with
draw and discard 100 mL from 1,000 mL chlorambucil).
NaCl bag. Withdraw 50 mL from 2 single-
Chronic Lymphocytic Leukemia
use 1,000-mg vials and add to
(Refractory)
bag. • Gently invert to mix.
Rate of administration • Dose 1:
IV infusion: ADULTS, ELDERLY: Recom-
Initiate infusion at rate of 3.6 mg/hr (12 mended dosage is 12 doses given on the
mL/hr). • Dose 2: Initiate infusion at following schedule: 300 mg initial dose
rate of 24 mg/hr (12 mL/hr). • Dose (dose 1), followed 1 wk later by 2,000
3–12: Initiate infusion at rate of 50 mg/ mg wkly for 7 doses (doses 2–8), fol-
hr (25 mL/hr). • If no infusion toxicity, lowed 4 wks later by 2,000 mg every 4
rate of infusion may be increased every wks for 4 doses (doses 9–12).
30 min, using following table: Chronic Lymphocytic Leukemia
(Relapsed)
Interval After Doses IV infusion: ADULTS, ELDERLY: 300 mg
Start of Dose 1 Dose 2 3–12 (mL/ once on day 1, then 1,000 mg on day 8,
Infusion (min) (mL/hr) (mL/hr) hr) then 1,000 mg on day 1 of subsequent O
0–30 12 12 25 28-day cycles for a maximum of 6 cycles
31–60 25 25 50 (in combination with fludarabine and
61–90 50 50 100
91–120 100 100 200
cyclophosphamide).
Over 120 200 200 400
Extended Treatment of CLL
Storage • Refrigerate vials. • After IV infusion: ADULTS, ELDERLY: 300 mg
dilution, solution should be used within once on day 1, then 1,000 mg on day 8,
first 12 hrs; discard preparation after 24 then 1,000 mg 7 wks later and q8wks
hrs. • Discard if discoloration is pres- thereafter up to a maximum of 2 yrs.
ent, but solution may contain visible,
Dosage in Renal/Hepatic Impairment
translucent-to-white particulates (will be
removed by in-line filter). No dose adjustment.

IV COMPATIBILITIES SIDE EFFECTS


Prepare all doses with 0.9% NaCl. Do not Frequent (20%–14%): Fever, cough, diar-
mix with dextrose solutions or any other rhea, fatigue, rash. Occasional (13%–
5%): Nausea, bronchitis, peripheral edema,
medications.
nasopharyngitis, urticaria, insomnia, head-
INDICATIONS/ROUTES/DOSAGE ache, sinusitis, muscle spasm, hypertension.
b ALERT c Premedicate 30 min to 2 ADVERSE EFFECTS/TOXIC
hrs before each infusion with acetamino- REACTIONS
phen, an antihistamine, and a corticoste-
roid as prophylaxis for infusion reaction. Most common serious adverse reactions
Flush IV line with 0.9% NaCl before and were bacterial, viral, fungal infections
after each dose. Interrupt infusion if (including pneumonia and sepsis), septic

Canadian trade name Non-Crushable Drug High Alert drug


854 OLANZapine
shock, neutropenia, thrombocytopenia. j BLACK BOX ALERT j
Infusion reactions occur more frequently Elderly pts with dementia-related
with first 2 infusions. Severe infusion psychosis are at increased risk for
mortality due to cerebrovascular
reactions manifested as angioedema, events. Sedation (including coma),
bronchospasm, dyspnea, fever, chills, delirium reported following use of
back pain, hypotension. Progressive mul- ZyPREXA Relprevv.
tifocal leukoencephalopathy may occur. Do not confuse OLANZapine
Small bowel obstruction has been noted. with olsalazine or QUEtiapine,
or ZyPREXA with CeleXA or
NURSING CONSIDERATIONS ZyrTEC.
BASELINE ASSESSMENT
FIXED-COMBINATION(S)
Screen pts at high risk of hepatitis B virus.
Symbyax: OLANZapine/FLUoxetine
Assess baseline CBC prior to therapy. Of-
(an antidepressant): 6 mg/25 mg,
fer emotional support.
6 mg/50 mg, 12 mg/25 mg, 12 mg/50
INTERVENTION/EVALUATION mg.
Monitor renal function, electrolytes. uCLASSIFICATION
Monitor CBC for evidence of myelosup-
pression during therapy, and increase PHARMACOTHERAPEUTIC: Second-
frequency of monitoring in pts who de- generation (atypical) antipsychotic.
velop Grade 3 or 4 cytopenia. Monitor CLINICAL: Antipsychotic.
for blood dyscrasias (fever, sore throat,
signs of local infection, unusual bruis- USES
ing/bleeding from any site), symptoms
of anemia (excessive fatigue, weakness). PO: Management of manifestations of
O Closely monitor for infusion reactions. schizophrenia. Treatment of acute mania
associated with bipolar I disorder as
PATIENT/FAMILY TEACHING monotherapy or in combination with
• Do not have immunizations without lithium or valproate. In combination
physician’s approval (lowers body’s resis- with FLUoxetine: treatment of depressive
tance). • Avoid contact with those who episodes associated with bipolar I disor-
have recently received live virus vac- der and treatment of treatment-resistant
cine. • Avoid crowds, those with infec- bipolar depression. Maintenance treat-
tion. • Promptly report fever, sore ment of bipolar I disorder. IM: ZyPREXA
throat, signs of infection. • Report symp- Intramuscular: Controls acute agitation
toms of infusion reactions (e.g., fever, in schizophrenia and bipolar mania. Rel-
chills, breathing problems, rash); bleed- prevv: Long-acting antipsychotic for IM
ing, bruising, petechiae, worsening weak- injection for treatment of schizophrenia.
ness or fatigue; new neurologic symptoms OFF-LABEL: Prevention of chemotherapy-
(e.g., confusion, loss of balance, vision induced nausea/vomiting. Acute treatment
problems); symptoms of hepatitis (e.g., of delirium. Treatment of anorexia ner-
fatigue, yellow discoloration of skin/eyes); vosa, Tourette’s syndrome, tic disorder.
worsening abdominal pain, nausea.
PRECAUTIONS
Contraindications: Hypersensitivity to
OLANZapine. Cautions: Disorders in
OLANZapine which CNS depression is prominent; car-
diac disease, hemodynamic instability,
oh-lan-za-peen prior MI, ischemic heart disease; hyper-
(Apo-OLANZapine , ZyPREXA, lipidemia, pts at risk for aspiration pneu-
ZyPREXA Relprevv, ZyPREXA Zydis) monia, decreased GI motility, urinary

underlined – top prescribed drug


OLANZapine 855
retention, BPH, narrow-angle glaucoma, Orally Disintegrating: (ZyPREXA Zydis): 5
diabetes, elderly, pts at risk for suicide, mg, 10 mg, 15 mg, 20 mg.
Parkinson’s disease, severe renal/hepatic
impairment, predisposition to seizures. ADMINISTRATION/HANDLING
PO
ACTION • Give without regard to food.
Antagonizes alpha1-adrenergic, DOPa-
mine, histamine, muscarinic, serotonin Orally Disintegrating
receptors. Produces anticholinergic, his- • Remove by peeling back foil (do not
taminic, CNS depressant effects. Thera- push through foil). • Place in mouth
peutic Effect: Diminishes psychotic immediately. • Tablet dissolves rapidly
symptoms through combined antagonism with saliva and may be swallowed with or
of dopamine and serotonin receptors. without liquid.

PHARMACOKINETICS IM (ZyPREXA Intramuscular)


Well absorbed after PO administration. • Reconstitute 10-mg vial with 2.1 mL
Rapid absorption following IM admin- Sterile Water for Injection to provide
istration. Protein binding: 93%. Widely concentration of 5 mg/mL. • Use within
distributed. Excreted in urine (57%), 1 hr following reconstitution. • Discard
feces (30%). Not removed by dialysis. unused portion.
Half-life: 21–54 hrs. IM (Relprevv)
LIFESPAN CONSIDERATIONS • Dilute to final concentration of 150
mg/mL. • Shake vigorously to mix.
Pregnancy/Lactation: Unknown if • Store at room temperature for up to
drug crosses placenta or is distributed 24 hrs.
in breast milk. Children: Safety and effi- O
cacy not established. Elderly: Use cau- INDICATIONS/ROUTES/DOSAGE
tion. Consider lower starting doses. Schizophrenia
INTERACTIONS Note: Discontinue gradually to avoid
withdrawal symptoms and reduce
DRUG: Alcohol, CNS depressants (e.g., relapse. PO: ADULTS, ELDERLY: Initially,
LORazepam, morphine, zolpidem) may 5–10 mg once daily. May increase to
increase CNS depressant effects. Anticholin- 10 mg/day within 5–7 days. If fur-
ergics (e.g., aclidinium, ipratropium, ther adjustments are indicated, may
tiotropium, umeclidinium) may increase increase by 5 mg/day at 7-day intervals.
anticholinergic effect. QT-prolonging Maintenance: 10–20 mg/day. Maxi-
agents (e.g., amiodarone, haloperidol, mum: 20 mg/day. CHILDREN 13 YRS AND
moxifloxacin, sotalol) may cause QT OLDER: Initially, 2.5–5 mg/day. Titrate
interval prolongation. HERBAL: Herbals in 2.5- or 5-mg increments at wkly
with sedative properties (e.g., chamo- intervals. Target dose: 10 mg. Maxi-
mile, kava kava, valerian) may increase mum: 20 mg/day.
CNS depression. FOOD: None known. LAB IM: (Long-Acting [Relprevv]): ADULTS,
VALUES: May increase serum GGT, choles- ESTABLISHED ON 10 MG/DAY ORALLY: 210
terol, prolactin, ALT, AST. mg q2wks for 4 doses or 405 mg q4wks
AVAILABILITY (Rx) for 2 doses. Maintenance: 150 mg
q2wks or 300 mg q4wks. ESTABLISHED
Injection, Powder for Reconstitution: ON 15 MG/DAY ORALLY: 300 mg q2wks for
(ZyPREXA): 10 mg. Suspension for IM 4 doses. Maintenance: 210 mg q2wks
Injection: (Relprevv): 210 mg, 300 mg, or 405 mg q4wks. ESTABLISHED ON 20 MG/
405 mg. Tablets: (ZyPREXA): 2.5 mg, 5 DAY ORALLY: 300 mg q2wks.
mg, 7.5 mg, 10 mg, 15 mg, 20 mg. Tablets,

Canadian trade name Non-Crushable Drug High Alert drug


856 OLANZapine
Depression Associated with Bipolar pharyngitis, visual changes (dim vision).
Disorder (with FLUoxetine) Rare: Tachycardia; back, chest, abdomi-
PO: ADULTS, ELDERLY: Initially, 5 mg in eve- nal, or extremity pain; tremor.
ning. May increase dose in 5 mg increments
at intervals of q1–7 days based on response ADVERSE EFFECTS/TOXIC
and tolerability up to 15 mg/day (adjunctive REACTIONS
therapy) or up to 20 mg/day (monotherapy). Rare reactions include seizures, neurolep-
CHILDREN 10–17 yrs: Initially, 2.5 mg once tic malignant syndrome, a potentially fatal
daily in evening. Adjust dose as tolerated. syndrome characterized by hyperpyrexia,
muscle rigidity, irregular pulse or B/P,
Treatment-Resistant Depression (with tachycardia, diaphoresis, cardiac arrhyth-
FLUoxetine) mias. Extrapyramidal symptoms (EPS),
PO: ADULTS, ELDERLY: Initially, 5 mg in dysphagia may occur. Overdose (300 mg)
evening. May gradually increase dose produces drowsiness, slurred speech.
based on response and tolerability up to
20 mg/day. Range: 5–20 mg/day. NURSING CONSIDERATIONS
Bipolar Mania BASELINE ASSESSMENT
PO: ADULTS, ELDERLY: (Monotherapy): Obtain baseline LFT, serum glucose,
Initially, 10–15 mg/day. May increase by weight, lipid profile before initiating
5 mg/day at intervals of at least 24 hrs. treatment. Assess behavior, appearance,
Range: 5–20 mg/day. Maximum: 20 mg/ emotional status, response to environ-
day. (In Combination with Lithium or ment, speech pattern, thought content.
Valproate): Initially, 10 mg/day. Range:
5–20 mg/day. CHILDREN 13 YRS OF AGE INTERVENTION/EVALUATION
AND OLDER: Initially, 2.5–5 mg/day. Adjust Monitor B/P, serum glucose, lipids, LFT.
O Assess for tremors, changes in gait, ab-
dose by 2.5–5 mg daily to target dose of 10
mg/day. Range: 2.5–20 mg/day. normal muscular movements, behavior.
Supervise suicidal-risk pt closely during
Dosage for Elderly, Debilitated Pts, Pts early therapy (as depression lessens,
Predisposed to Hypotensive Reactions energy level improves, increasing sui-
Initial dosage: 5 mg/day. cide potential). Assess for therapeutic
response (interest in surroundings, im-
Control of Agitation provement in self-care, increased ability
IM: ADULTS, ELDERLY: (Short-Acting): to concentrate, relaxed facial expression).
Initially, 5–10 mg. Additional doses (up Assist with ambulation if dizziness occurs.
to 10 mg) may be considered. However, Assess sleep pattern. Notify physician if ex-
allow at least 2 hrs (after initial dose) trapyramidal symptoms (EPS) occur.
or 4 hrs (after second dose) to evaluate
response. Maximum: 30 mg/day. PATIENT/FAMILY TEACHING
• Avoid dehydration, particularly during ex-
Dosage in Renal/Hepatic Impairment ercise, exposure to extreme heat, concurrent
No dose adjustment. use of medication causing dry mouth, other
SIDE EFFECTS drying effects. • Sugarless gum, sips of wa-
ter may relieve dry mouth. • Report sus-
Frequent (26%–10%): Drowsiness, agita- pected pregnancy. • Take medication as
tion, insomnia, headache, nervousness, prescribed; do not stop taking or increase
hostility, dizziness, rhinitis. Occasional dosage. • Slowly go from lying to stand-
(9%–5%): Anxiety, constipation, nonag- ing. • Avoid alcohol. • Avoid tasks that
gressive atypical behavior, dry mouth, require alertness, motor skills until response
weight gain, orthostatic hypotension, to drug is established. • Monitor diet, exer-
fever, arthralgia, restlessness, cough, cise program to prevent weight gain.
underlined – top prescribed drug
olaparib 857

LIFESPAN CONSIDERATIONS
olaparib Pregnancy/Lactation: Avoid preg-
oh-lap-a-rib nancy; may cause fetal harm. Females of
(Lynparza) reproductive potential should use effec-
tive contraception during treatment and
uCLASSIFICATION for at least 6 mos after discontinuation.
PHARMACOTHERAPEUTIC: PARP Unknown if distributed in breast milk.
inhibitor. CLINICAL: Antineoplastic. Must either discontinue drug or discon-
tinue breastfeeding. Children: Safety
and efficacy not established. Elderly: No
age-related precautions noted.
USES
Capsules/Tablets: Treatment of delete- INTERACTIONS
rious or suspected deleterious germline DRUG: Strong CYP3A inhibitors
BRCA-mutated advanced ovarian cancer (e.g., clarithromycin, ketoconazole,
in pts who have been treated with three ritonavir), moderate CYP3A inhibi-
or more prior lines of chemotherapy. tors (e.g., atazanavir, ciprofloxa-
Tablets only: Maintenance treatment cin) may increase concentration/effect.
of adults with recurrent epithelial ovar- Strong CYP3A inducers (e.g., carBA-
ian, fallopian tube or primary peritoneal Mazepine), moderate CYP3A induc-
cancer who are in complete or partial ers (e.g., nafcillin) may decrease
response to platinum-based chemo- concentration/effect. HERBAL: Bitter
therapy. Treatment of germline BRCA- orange may increase concentration/
mutated, HER2-negative metastatic breast effect. FOOD: Grapefruit products,
cancer in pts who have been treated with Seville oranges may increase concen-
chemotherapy. tration/effect. High-fat food may delay O
absorption. LAB VALUES: May increase
PRECAUTIONS mean corpuscular volume, serum cre-
Contraindications: Hypersensitivity to atinine. May decrease Hct, Hgb, lympho-
olaparib. Cautions: Baseline anemia, cytes, neutrophils, RBC.
neutropenia, lymphopenia, thrombocy-
topenia. History of pulmonary disease. AVAILABILITY (Rx)
Avoid concomitant use of strong or mod- Capsules: 50 mg. Tablets: 100 mg, 150
erate CYP3A inhibitors, strong or moder- mg.
ate CYP3A inducers.
ADMINISTRATION/HANDLING
ACTION PO
Inhibits poly (ADP-ribose) polymerase Capsules: • Give without regard to
(PARP) enzymes, involved in normal cel- food. • Administer capsules whole; do
lular hemostasis (e.g., DNA transcription, not break, cut, crush, or open. Tablets:
cell cycle regulation, and DNA repair). May give with or without food. Administer
Disrupts cellular homeostasis, resulting in tablet whole; do not break, cut, crush, or
cell death. Therapeutic Effect: Inhibits divide.
tumor cell growth and metastasis.
INDICATIONS/ROUTES/DOSAGE
PHARMACOKINETICS Note: Do not substitute tablets with cap-
Rapidly absorbed. Metabolized in liver. sules on a mg to mg basis.
Protein binding: 82%. Peak plasma con-
centration: 1–3 hrs. Steady-state con- Ovarian Cancer
centration: 3–4 days. Excreted in urine PO: ADULTS, ELDERLY: (Capsule): 400 mg
(44%), feces (42%). Half-life: 11.9 hrs. twice daily. Continue until disease
Canadian trade name Non-Crushable Drug High Alert drug
858 olaparib
progression or unacceptable toxicity. If ADVERSE EFFECTS/TOXIC
a dose is missed, give next dose at its REACTIONS
scheduled time. (Tablet): 300 mg (2 × Myelodysplastic syndrome/acute myeloid
150 mg) twice daily (100-mg tablets leukemia reported in 2% of pts. Pneu-
available for dose reduction). Mainte- monitis, including fatal cases, occurred
nance: (Tablets only): 300 mg (2 × in less than 1% of pts. Respiratory tract
150 mg) twice daily (100-mg tablets infections including nasopharyngitis,
available for dose reduction). Pts with pharyngitis, upper respiratory tract infec-
complete response at 2 yrs should dis- tion occurred in 43% of pts.
continue treatment. Pts with evidence of
disease at 2 yrs may continue treatment NURSING CONSIDERATIONS
beyond 2 yrs.
BASELINE ASSESSMENT
Breast Cancer (metastatic, HER2-negative, Obtain baseline CBC. Do not initiate
BRCA-mutated) therapy until pts have recovered from he-
PO: ADULTS, ELDERLY: (Tablet): 300 mg matologic toxicities caused by previous
(2 × 150 mg) twice daily. Continue until chemotherapy. Question history of pul-
disease progression or unacceptable monary disease. Receive full medication
toxicity. history and screen for interactions. Offer
emotional support.
Dose Modification
Dose Reduction for Adverse Reactions INTERVENTION/EVALUATION
PO: ADULTS, ELDERLY: Interrupt treat- Monitor CBC monthly. For prolonged he-
ment until resolved. Then, decrease to matologic toxicities, interrupt treatment
200 mg twice daily. If further dose reduc- and monitor CBC wkly until recovery. If
O tion is indicated, decrease to 100 mg hematologic levels have not recovered to
twice daily. CTCAE Grade 1 or 0 after 4 wks of treat-
Concomitant Use of Strong CYP3A ment interruption, consider hematology
Inhibitors consultation for further investigations
PO: ADULTS, ELDERLY: 150 mg twice such as bone marrow analysis and blood
daily. sample for cytogenetics. Monitor for my-
Concomitant Use of Moderate CYP3A elodysplastic syndrome/acute myeloid
Inhibitors leukemia, pneumonitis.
PO: ADULTS, ELDERLY: 200 mg twice
daily. PATIENT/FAMILY TEACHING
• Report bleeding or bruising easily,
Dosage in Renal Impairment bloody urine or stool, frequent infections,
Mild impairment: No dose adjust- fatigue, shortness of breath, weakness,
ment. Moderate to severe impair- weight loss; may indicate acute bone mar-
ment: Not specified; use caution. row suppression or acute leukemia. •
Report new or worsening respiratory symp-
Dosage in Hepatic Impairment toms such as cough, difficulty breathing,
Not specified; use caution. fever, wheezing; may indicate severe lung
inflammation. • Do not ingest grapefruit
SIDE EFFECTS
product, Seville oranges. • Do not take
Frequent (66%–21%): Fatigue, asthenia, herbal products. • Avoid pregnancy;
nausea, vomiting, abdominal pain, diar- treatment may cause birth defects or mis-
rhea, dyspepsia, decreased appetite, carriage. Do not breastfeed. Females of
headache, back pain, rash, myalgia, childbearing potential should use effective
arthralgia, musculoskeletal pain, dysgeu- contraception during treatment and for at
sia, cough. least 6 mos after stopping therapy.

underlined – top prescribed drug


olaratumab 859
discontinuation. Unknown if distrib-
olaratumab uted in breast milk. Breastfeeding not
recommended during treatment and
oh-lar-at-ue-mab for at least 3 mos after discontinua-
(Lartruvo) tion. Children: Safety and efficacy not
Do not confuse olaratumab with established. Elderly: Not specified; use
elotuzumab, obinutuzumab. caution.
uCLASSIFICATION INTERACTIONS
PHARMACOTHERAPEUTIC: Platelet- DRUG: May decrease therapeutic effect
derived growth factor receptor of BCG (intravesical). HERBAL: None
(PDGFR) alpha blocker. Monoclonal significant. FOOD: None known. LAB
antibody. CLINICAL: Antineoplastic. VALUES: May increase serum alkaline
phosphatase, glucose. May decrease lym-
phocytes, neutrophils, platelets; serum
USES
phosphate, potassium, magnesium. May
Treatment of adult pts with soft tissue prolong aPTT.
sarcoma (STS), in combination with
doxorubicin, with a histologic subtype AVAILABILITY (Rx)
for which an anthracycline-containing Injection Solution: 190 mg/19 mL, 500
regimen is appropriate and which is not mg/50 mL.
amendable to curative treatment with
radiotherapy or surgery. ADMINISTRATION/HANDLING
PRECAUTIONS IV
Contraindications: Hypersensitivity to Preparation • Visually inspect for O
olaratumab. Cautions: Electrolyte imbal- particulate matter or discoloration. Solu-
ance, pts at risk for hyperglycemia (e.g., tion should appear clear to slightly opal-
diabetes, recent surgery, chronic use of escent, colorless to slightly yellow in
corticosteroids). color. • Do not use if solution is cloudy,
discolored, or if visible particles are
ACTION observed. • Withdraw required dose
A human IgG-1 antibody that binds to from vial and dilute into 250 mL 0.9%
PDGFR-alpha. Blocks receptor activation and NaCl bag. • Mix by gently inver-
disrupts PDGF receptor signaling. PDGFR sion. • Do not shake or agitate. • Dis-
alpha receptor plays a role in cell differentia- card used portions from vial.
tion, growth, and angiogenesis. Therapeu- Infusion guidelines • Do not give
tic Effect: Exhibits antitumor activity. IV push or bolus. • Do not mix or
infuse with other medications, electro-
PHARMACOKINETICS lytes. • Flush IV line with 0.9% NaCl
Widely distributed. Metabolism not after completion of infusion.
specified. Excretion not specified. Half- Rate of administration • Infuse over
life: 11 days (range: 6–24 days). 60 min via dedicated IV line.
Storage • May refrigerate diluted
LIFESPAN CONSIDERATIONS solution up to 24 hrs or store at room
Pregnancy/Lactation: Avoid preg- temperature for up to 4 hrs (includes
nancy; may cause fetal harm/malforma- infusion time). • Do not freeze. • If
tions. Females of reproductive potential diluted solution is refrigerated, allow to
must use effective contraception dur- warm to room temperature before
ing treatment and up to 3 mos after administration. • Discard solution if

Canadian trade name Non-Crushable Drug High Alert drug


860 olaratumab
not administered within required time ADVERSE EFFECTS/ TOXIC
frame. REACTIONS
Neutropenia, lymphopenia, thrombo-
IV INCOMPATIBILITIES
cytopenia are expected responses to
Do not dilute in dextrose-containing therapy. Life-threatening infusion-related
solutions. reactions including anaphylaxis, bron-
chospasm, cardiac arrest, chills, dys-
INDICATIONS/ROUTES/DOSAGE
pnea, hypotension, pyrexia occurred in
Note: Premedicate with diphenhydr- 14% of pts. CTCAE Grade 3 or 4 infusion-
amine 25–50 mg IV and dexamethasone related reactions occurred in 2% of pts.
10–20 mg IV on day 1 of cycle 1. Immunogenicity (auto anti-olaratumab
Soft Tissue Sarcoma antibodies) reported in 3.5% of pts.
IV: ADULTS, ELDERLY: 15 mg/kg on days NURSING CONSIDERATIONS
1 and 8 of each 21-day cycle. Adminis-
ter with doxorubicin for the first 8 cycles BASELINE ASSESSMENT
(see manufacturer guidelines). After 8 Obtain ANC, CBC, BMP. Obtain pregnancy
cycles are completed, continue olara- test in females of reproductive poten-
tumab as a single agent. Continue until tial. Question history of hypersensitivity
disease progression or unacceptable reactions, infusion-related reactions;
toxicity. diabetes. Ensure that proper resuscitative
Dose Modification equipment, medications are readily avail-
Infusion Reaction able (e.g., albuterol, antipyretics, antihis-
CTCAE Grade 1 or 2 infusion reac- tamines, epinephrine; isotonic IV fluids;
tion: Interrupt infusion until symptoms bag-valve mask, oxygen, rapid sequence
O resolve, then resume infusion at 50% of intubation kit). Assess nutritional/hydra-
the initial infusion rate. CTCAE Grade tion status. Offer emotional support.
3 or 4 infusion reaction: Immediately
INTERVENTION/EVALUATION
stop infusion; do not restart.
Neutropenia Monitor ANC, CBC for neutropenia,
Neutropenic fever/infection; CTCAE lymphopenia, thrombocytopenia; BMP
Grade 4 neutropenia lasting greater for electrolyte imbalance; vital signs.
than 1 wk: Withhold treatment until Diligently monitor for infusion-related
ANC 1000 cells/mm3 or greater, then reactions. If severe or life-threatening re-
reduce dose to 12 mg/kg. Do not actions occur, immediately stop infusion
increase dose for subsequent infusions. and provide appropriate medical sup-
port. Due to risk of respiratory compro-
Dosage in Renal/Hepatic Impairment mise, pts with bronchospasm, dyspnea,
Not specified; use caution. hypoxia should be given immediate sup-
plemental oxygen, hypersensitivity medi-
SIDE EFFECTS cations, hemodynamic support. Mild to
Frequent (73%–22%): Nausea, fatigue, moderate infusion reactions may require
asthenia, musculoskeletal pain, interruption of infusion, decrease of in-
arthralgia, back pain, bone pain, flank fusion rate, symptom management. Offer
pain, groin pain, musculoskeletal chest antiemetic if nausea, vomiting occurs.
pain, myalgia, muscle spasm, neck Monitor daily pattern of bowel activity,
pain, extremity pain, mucositis, alo- stool consistency.
pecia, vomiting, diarrhea, decreased
appetite, abdominal pain, neuropathy. PATIENT/FAMILY TEACHING
Occasional (20%–11%): Headache, anxi- • Life-threatening infusion reactions, al-
ety, dry eyes. lergic reactions, cardiac arrest may
underlined – top prescribed drug
olmesartan 861
o­ ccur during infusion. Immediately re- USES
port difficulty breathing, chest pain, chest Treatment of hypertension alone or in
tightness, chills, dizziness, fast heart rate, combination with other antihypertensives.
fever, flushing, headache, hives, itching,
low blood pressure, nausea, throat pain PRECAUTIONS
or swelling, rash. • Treatment may de- Contraindications: Hypersensitivity to
press your immune system and reduce olmesartan. Concomitant use with aliski-
your ability to fight infection. Report ren in pts with diabetes. Cautions: Renal
symptoms of infection such as body impairment, unstented unilateral or bilat-
aches, burning with urination, chills, eral renal arterial stenosis, significant aor-
cough, fatigue, fever. Avoid those with tic/mitral stenosis. Concurrent potassium
active infection. • Females of child- supplements; pts who are volume depleted.
bearing potential should use effective
contraception during treatment and for ACTION
at least 3 mos after last dose. Do not Blocks vasoconstrictor, aldosterone-
breastfeed. • Generalized pain is an ex- secreting effects of angiotensin II by
pected side effect. • Treatment may inhibiting binding of angiotensin II to
cause severe diarrhea. Drink plenty of AT1 receptors in vascular smooth muscle.
fluids. • Hair loss is an expected side Therapeutic Effect: Causes vasodila-
effect of therapy. tion, decreases peripheral resistance,
decreases B/P.
PHARMACOKINETICS
olmesartan Moderately absorbed after PO adminis-
tration. Hydrolyzed in GI tract to olme-
ol-me-sar-tan sartan. Protein binding: 99%. Excreted in O
(Benicar, Olmetec ) urine (35%–50%), remainder in feces.
j BLACK BOX ALERT jMay Not removed by hemodialysis. Half-
cause fetal injury, mortality. Dis- life: 13 hrs.
continue as soon as possible once
pregnancy is detected.
LIFESPAN CONSIDERATIONS
Do not confuse Benicar with
Mevacor. Pregnancy/Lactation: Unknown if dis-
tributed in breast milk. Children: Safety
FIXED-COMBINATION(S) and efficacy not established in children
Azor: olmesartan/amLODIPine (cal- younger than 6 yrs of age. Elderly: No
cium channel blocker): 20 mg/5 age-related precautions noted.
mg, 40 mg/5 mg, 20 mg/10 mg, 40 INTERACTIONS
mg/10 mg. Benicar HCT: olmesartan/
hydroCHLOROthiazide (a diuretic): DRUG: NSAIDs (e.g., ibuprofen,
20 mg/12.5 mg, 40 mg/12.5 mg, 40 naproxen) may decrease antihyperten-
mg/25 mg. Tribenzor: olmesartan/hy- sive effect. Aliskiren may increase hyper-
droCHLOROthiazide/amLODIPine: 20 kalemic effect. May increase adverse effects
mg/12.5 mg/5 mg, 40 mg/12.5 mg/5 of ACE inhibitors (e.g., benazepril,
mg, 40 mg/25 mg/5 mg, 40 mg/12.5 lisinopril). HERBAL: Herbals with
mg/10 mg, 40 mg/25 mg/10 mg. hypertensive properties (e.g., licorice,
yohimbe) or hypotensive properties
uCLASSIFICATION (e.g., garlic, ginger, ginkgo biloba)
PHARMACOTHERAPEUTIC: Angio- may alter effects. FOOD: None known. LAB
tensin II receptor antagonist. CLINI- VALUES: May slightly decrease Hgb, Hct.
CAL: Antihypertensive. May increase serum BUN, creatinine, bili-
rubin, ALT, AST.
Canadian trade name Non-Crushable Drug High Alert drug
862 olodaterol

AVAILABILITY (Rx) PATIENT/FAMILY TEACHING


Tablets: 5 mg, 20 mg, 40 mg. • Maintain adequate hydration. • Avoid
pregnancy. • Avoid tasks that require
ADMINISTRATION/HANDLING alertness, motor skills until response to
PO drug is established (possible dizziness
• Give without regard to food. effect). • Report any signs of infection
(sore throat, fever). • Therapy requires
INDICATIONS/ROUTES/DOSAGE lifelong control, diet, exercise.
Hypertension
PO: ADULTS, ELDERLY: Initially, 20 mg/
day. May increase to 40 mg/day after 2
wks. Lower initial dose may be necessary olodaterol
in pts receiving volume-depleting medica-
tions (e.g., diuretics). CHILDREN 6–16 YRS, oh-loe-da-ter-ol
WEIGHING 20 TO LESS THAN 35 KG: Initially, (Striverdi Respimat)
10 mg once daily. Range: 10–20 mg once j BLACK BOX ALERT jLong-
daily. WEIGHING 35 KG OR MORE: Initially, acting beta2-adrenergic agonists
20 mg once daily. Range: 20–40 mg once (LABA) increase risk of asthma-
related deaths. Not indicated for
daily. Use with caution. treatment of asthma.
Dosage in Renal/Hepatic Impairment
Do not confuse olodaterol with
Use caution. albuterol, indacaterol, formo-
terol, or salmeterol.
SIDE EFFECTS
FIXED-COMBINATION(S)
Occasional (3%): Dizziness. Rare (less
O than 2%): Headache, diarrhea, upper
Stiolto Respimat: olodaterol/tiotro-
respiratory tract infection. pium (bronchodilator): 2.5 mcg/2.5
mcg.
ADVERSE EFFECTS/TOXIC
uCLASSIFICATION
REACTIONS
Overdosage may manifest as hypoten- PHARMACOTHERAPEUTIC: Sympa-
sion, tachycardia. Bradycardia occurs thomimetic (beta2-adrenergic ago-
less often. Rare cases of rhabdomyolysis nist). CLINICAL: Bronchodilator.
have been reported.
USES
NURSING CONSIDERATIONS
Long-term, once-daily maintenance bron-
BASELINE ASSESSMENT chodilator treatment of airflow obstruction
Obtain B/P, apical pulse immediately in pts with chronic obstructive pulmonary
before each dose in addition to regular disease (COPD), including chronic bron-
monitoring (be alert to fluctuations). If chitis and emphysema. Not indicated in
excessive reduction in B/P occurs, place asthma, acute deterioration of COPD.
pt in supine position, feet slightly elevated.
Question for possibility of pregnancy. As- PRECAUTIONS
sess medication history (esp. diuretics). Contraindications: Hypersensitivity
to olodaterol. Asthma without use of
INTERVENTION/EVALUATION long-term asthma control medication,
Maintain hydration. Assess for evidence history of hypersensitivity to sympatho-
of upper respiratory infection. Assist with mimetics. Cautions: Diabetes, keto-
ambulation if dizziness occurs. Monitor acidosis, cardiovascular disorders (e.g.,
serum potassium level. Assess B/P for hy- coronary insufficiency, arrhythmias,
pertension, hypotension. hypertension, hypertrophic obstructive
underlined – top prescribed drug
olodaterol 863
cardiomyopathy), seizure disorder, long as possible. (See manufacturer
hyperthyroidism; history of severe bron- guidelines for priming instructions and
chospasm, long QT syndrome, electrolyte further information.)
imbalance.
INDICATIONS/ROUTES/DOSAGE
ACTION COPD
Stimulates beta2-adrenergic receptors in Inhalation: ADULTS, ELDERLY: Two
lungs, resulting in relaxation of bronchial inhalations (2.5 mcg per inhalation for
smooth muscle. Therapeutic Effect: total of 5 mcg) once daily, at same time
Relieves bronchospasm, reduces airway each day. Maximum: 5 mcg within
resistance, improves bronchodilation. 24-hr period.
PHARMACOKINETICS Dosage in Renal Impairment
Rapidly absorbed following inhalation. No dose adjustment.
Extensively distributed in tissue. Metab-
Dosage in Hepatic Impairment
olized in liver. Protein binding: 60%.
Mild to moderate impairment: No
Peak plasma concentration: 10–20 min.
Excreted in urine. Half-life: 45 hrs. dose adjustment. Severe impair-
ment: Use caution.
LIFESPAN CONSIDERATIONS
SIDE EFFECTS
Pregnancy/Lactation: Excretion into
Occasional (11%–4%): Nasopharyngi-
breast milk is probable. Breastfeeding
not recommended. May interfere with tis, upper respiratory tract infection,
uterine contractility. Children: Safety bronchitis, cough, back pain. Rare (3%–
2%): Dizziness, insomnia, dry mouth,
and efficacy not established. Elderly: No
age-related precaution noted. arthralgia, urinary retention. O
INTERACTIONS ADVERSE EFFECTS/TOXIC
REACTIONS
DRUG: Beta blockers (e.g., meto­
prolol) may decrease therapeutic effect, Life-threatening asthma-related events,
ca­use bronchospasms. Beta2-adrenergic bronchospasm, or worsening of COPD-
agonists (e.g., salmeterol) may related symptoms have been reported.
potentiate sympathomimetic effects. Serious cardiovascular events including
Linezolid may increase hyperten- arrhythmias, angina pectoris, cardiac
sive effect. HERBAL: None significant. arrest, hypertension, tachycardia; flat-
FOOD: None known. LAB VALUES: May
tening of T wave, prolongation of QTc
increase serum glucose. May decrease interval, ST segment depression have
serum potassium. occurred. All beta-adrenergic agonists
carry risk of hyperglycemia or significant
AVAILABILITY (Rx) hypokalemia. Pts with severe COPD or
Inhalation Spray (2.5 mcg/actuation): 28 hypokalemia have additional increased
metered actuations/cartridge with risk of adverse effects related to hypoxia
inhaler, 60 metered actuations/cartridge and concomitant medications.
with inhaler. NURSING CONSIDERATIONS
ADMINISTRATION/HANDLING BASELINE ASSESSMENT
Inhalation Obtain ABG, capillary glucose, O2 satura-
tion, serum potassium level, vital signs;
• While taking slow, deep breath ECG, pulmonary function test if appli-
through the mouth, press and release cable. Assess respiratory rate, depth,
button and continue slow inhalation as rhythm. Assess lung sounds for ­wheezing,
Canadian trade name Non-Crushable Drug High Alert drug
864 omacetaxine
rales. Receive full medication history PRECAUTIONS
and screen for drug interactions. Ques- Contraindications: Hypersensitivity to
tion history of asthma, cardiovascular omacetaxine. Cautions: Glucose intoler-
disease, diabetes, long QT syndrome, ance, poorly controlled diabetes, elderly,
seizure disorder. Teach proper inhaler recent GI bleeding. Avoid all use of antico-
priming and administration techniques. agulants, aspirin, NSAIDs; all pts with base-
INTERVENTION/EVALUATION line platelets less than 50,000 cells/mm3.
Routinely monitor capillary glucose, ACTION
O2 saturation, serum potassium level,
Inhibits protein synthesis of Bcr-Abl
vital signs. Auscultate lung sounds. Ob-
tyrosine kinase, a translocation-created
tain ECG for palpitation, tachycardia;
enzyme, created by the Philadelphia
symptomatic hypokalemia. Recommend
chromosome abnormality noted in
discontinuation of short-acting beta2-
chronic myeloid leukemia (CML). Ther-
agonists (use only for symptomatic relief
apeutic Effect: Inhibits tumor prolifer-
of acute respiratory symptoms). Monitor
ation and growth during accelerated and
for hypoglycemia.
chronic stages of CML.
PATIENT/FAMILY TEACHING
• Refill prescription when dose indicator
PHARMACOKINETICS
on left of inhaler reaches red area of Rapidly absorbed following SQ administra-
scale. • Follow manufacturer guidelines tion. Maximum concentration: 30 min.
for proper use of inhaler. • Drink plenty Protein binding: Less than 50%. Hydrolyzed
of fluids (decreases lung secretion viscos- via plasma esterases. Half-life: 6 hrs.
ity). • Rinse mouth with water after in-
halation to decrease mouth/throat irrita-
LIFESPAN CONSIDERATIONS
O Pregnancy/Lactation: May cause fetal
tion. • Avoid excessive use of caffeine
derivatives (chocolate, coffee, tea, harm. Not recommended in nursing
cola). • Report fever, productive cough, mothers. Unknown if distributed in
body aches, difficulty breathing; may indi- breast milk. Children: Safety and effi-
cate lung infection or worsening of COPD. cacy not established. Elderly: Increased
risk for toxicity (e.g., hematologic).
INTERACTIONS
omacetaxine DRUG: NSAIDs (e.g., ibuprofen, keto­
rolac, naproxen), anticoagulants
oh-ma-se-tax-een (e.g., heparin, warfarin), aspirin,
(Synribo) antiplatelets (e.g., clopidogrel) may
increase risk for bleeding. HERBAL: Echi-
uCLASSIFICATION nacea may decrease levels/effects.
PHARMACOTHERAPEUTIC: Protein FOOD: None known. LAB VALUES: May
synthesis inhibitor. CLINICAL: Anti- decrease platelets, Hgb, Hct, leukocytes,
neoplastic. lymphocytes. May increase serum ALT.

AVAILABILITY (Rx)
USES Injection, Powder for Reconstitution: 3.5-
Treatment of adult pts with chronic mg vial.
or accelerated phase chronic myeloid
leukemia (CML) with resistance and/ ADMINISTRATION/HANDLING
or intolerance to two or more tyrosine b ALERT c Must be administered by
kinase inhibitors. health care workers trained in proper

underlined – top prescribed drug


omacetaxine 865
chemotherapy handling and disposal (20%–11%): Headache, arthralgia, cough,
procedures. epistaxis, alopecia, constipation, abdom-
inal pain, peripheral edema, vomiting,
SQ
back pain, insomnia, rash.
Reconstitution • Reconstitute with 1
mL 0.9% NaCl. • Gently swirl until pow- Accelerated Phase
der is completely dissolved. • Inspect Occasional (19%–7%): Diarrhea, nau-
vial for particular matter or discolor- sea, fatigue, pyrexia, asthenia, vomiting,
ation. • Reconstituted vial will provide cough, abdominal pain, chills, anorexia,
a concentration of 3.5 mg/mL. • Avoid headache. Rare (7% or less): Dyspnea,
contact with skin. epistaxis.
Storage • Solution should appear
clear. • May store solution at room ADVERSE EFFECTS/TOXIC
temperature for up to 12 hrs or may REACTIONS
refrigerate up to 24 hrs. • Discard Thrombocytopenia, neutropenia, leuko-
unused solution. penia, lymphopenia, or myelosuppres-
sion is an expected response to therapy,
INDICATIONS/ROUTES/DOSAGE but more severe reactions including bone
Note: If dose is missed, skip dose and marrow failure, febrile neutropenia may
resume next regularly scheduled dose. result in life-threatening events. Pts with
neutropenia are at increased risk for infec-
Chronic or Accelerated Myeloid Leukemia
tion. Thrombocytopenia may increase risk
SQ: ADULTS, ELDERLY: Induction dose:
for intracranial hemorrhage, GI bleeding.
1.25 mg/m2 twice daily for 14 consecu- Hyperglycemic events including hypergly-
tive days every 28 days, over 28-day cycle. cemic hyperosmolar nonketotic syndrome
Continue induction dose until hemato- (HHNK) may occur. Pts with uncontrolled
logic response achieved. Maintenance O
diabetes are at increased risk for hypergly-
dose: 1.25 mg/m2 twice daily for 7 con- cemic emergency.
secutive days every 28 days of a 28-day
cycle. Continue until no longer achieving NURSING CONSIDERATIONS
clinical treatment benefit.
BASELINE ASSESSMENT
Dosage Modification Obtain baseline serum chemistries, CBC,
Hematologic toxicity: If neutrophils PT/INR if on anticoagulants. Question for
less than 500 cells/mm3 or platelets less possibility of pregnancy, current breast-
than 50,000 cells/mm3, interrupt therapy. feeding status. Obtain negative urine
Restart when neutrophil count greater pregnancy before initiating treatment.
than or equal to 1000 cells/mm3 or platelet Obtain full medication history including
count greater than or equal to 50,000 cells/ herbal products, anticoagulants. Ques-
mm3 and reduce number of dosing days tion for history of diabetes, GI bleed-
by 2. Nonhematologic toxicity: Inter- ing. Offer emotional support.
rupt therapy until toxicity/adverse effects
resolved. Continue indefinitely until pt no INTERVENTION/EVALUATION
longer benefits from therapy. Monitor CBC wkly, then q2wks during
maintenance phase. Obtain frequent
Dosage in Renal/Hepatic Impairment blood glucose levels, especially in dia-
No dose adjustment. betic pts. Do not initiate therapy until
SIDE EFFECTS negative urine pregnancy confirmed.
Monitor LFT if hepatic impairment sus-
Chronic Phase pected. If drug exposure occurs, imme-
Frequent (45%–25%): Diarrhea, nausea, diately wash affected area with soap and
fatigue, pyrexia, asthenia. Occasional

Canadian trade name Non-Crushable Drug High Alert drug


866 omadacycline
water. Consider isolation protocol if pt organisms: Staphylococcus aureus
develops neutropenia. (methicillin-susceptible and -resistant
isolates), Staphylococcus lugdunen-
PATIENT/FAMILY TEACHING
sis, Streptococcus anginosus group
• Report if pregnant or planning to be- (including S. anginosus, S. interme-
come pregnant. • Use barrier methods dius, S. constellatus), Enterococcus
during sexual activity. • Strictly avoid faecalis, Enterobacter cloacae, and
pregnancy. • May cause male infertil- Klebsiella pneumoniae.
ity. • Immediately report yellowing of
skin or eyes, abdominal pain, bruising, PRECAUTIONS
black/tarry stools, dark urine, dehydra- Contraindications: Hypersensitivity to
tion, GI bleeding, nausea, vomiting, omadacycline, other tetracyclines. Cau-
rash. • Report fever, cough, night tions: History or predisposition to can-
sweats, flu-like symptoms, skin didiasis infection; recent Clostridium
changes. • Shortness of breath, pale difficile infection or antibiotic-associ-
skin, weakness may indicate bleeding or ated colitis; history of pancreatitis. Avoid
severe myelosuppression. • Avoid tasks use during pregnancy or during tooth
that require alertness, motor skills until development in children.
response to drug is established.
ACTION
Inhibits bacterial protein synthesis by
binding to 30S ribosomal subunit. Ther-
omadacycline apeutic Effect: Bacteriostatic.
oh-mad-a-sye-kleen PHARMACOKINETICS
O (Nuzyra) Widely distributed. Not systemically
Do not confuse omadacycline metabolized. Protein binding: 20%.
with doxycycline, minocycline, Excreted in feces (76%–84%), urine
tigecycline, or tetracycline, (14%). Half-life: 13.5–16.8 hrs.
or Nuzyra with Ampyra or
Lucemyra. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Avoid preg-
uCLASSIFICATION
nancy; may cause fetal harm. Female
PHARMACOTHERAPEUTIC: Tetracy- pts of reproductive potential should use
cline. CLINICAL: Antibiotic. effective contraception during treat-
ment. Fetal tooth discoloration, enamel
hypoplasia, inhibited bone growth may
USES occur in neonates when given in second
Treatment of adults with community- or third trimester. Unknown if distrib-
acquired bacterial pneumonia (CABP) uted in breast milk or crosses the pla-
caused by susceptible organisms: Strep- centa; however, other tetracyclines are
tococcus pneumoniae, Staphylococ- secreted in breast milk and are known
cus aureus (methicillin-susceptible to cross the placenta. Breastfeeding not
isolates), Haemophilus influenzae, recommended during treatment and up
Haemophilus parainfluenzae, Kleb- to 4 days after discontinuation. Chil-
siella pneumoniae, Legionella pneu- dren: Safety and efficacy not established
mophila, Mycoplasma pneumoniae, in pts 8 yrs and younger. Elderly: May
and Chlamydophila pneumoniae. have increased risk of treatment-related
Treatment of adults with acute bac- mortality imbalance when adminis-
terial skin and skin structure infec- tered for community-acquired bacterial
tions (ABSSSI) caused by susceptible pneumonia.

underlined – top prescribed drug


omadacycline 867

INTERACTIONS Storage • Store unused vials at room


DRUG: Antacids containing alumi- temperature. • May refrigerate diluted
num, calcium, magnesium; bismuth solution for up to 7 days or store at room
subsalicylate, iron preparations, temperature for no more than 12 hrs.
multivitamins, bile acid sequestrants
IV INCOMPATABILITIES
(e.g., cholestyramine), sucralfate
may decrease absorption/concentration. Do not mix with infusion solutions con-
HERBAL: None significant. FOOD: Food, taining multivalent cations (e.g., calcium,
dairy products decrease absorption/ magnesium).
concentration. LAB VALUES: May increase
INDICATIONS/ROUTES/DOSAGE
serum ALT, AST. May decrease Hgb.
Community-Acquired Bacterial
AVAILABILITY (Rx) Pneumonia
Tablets: 150 mg. Injection, Powder for Note: An initial IV loading dose is
Reconstitution: 100 mg. recommended.
IV/PO: ADULTS, ELDERLY: 200 mg IV on
ADMINISTRATION/HANDLING day 1 or 100 mg twice on day 1 (as load-
PO ing dose). Maintenance: 100 mg IV
• Give with water after pt has fasted for once daily or 300 mg PO once daily for
at least 4 hrs. No food or drink (except 7–14 days.
water) may be consumed for at least 2
Acute Bacterial Skin/Skin Structure
hrs after administration. • Do not give
Infections
multivitamins, antacid, or dairy products
IV: ADULTS, ELDERLY: 200 mg on day 1 or
for at least 4 hrs.
100 mg twice on day 1 (as loading dose).
IV Maintenance: 100 mg once daily for O
Reconstitution • Calculate the num- 7–14 days.
ber of vials required for dose (2 vials for PO: ADULTS, ELDERLY: 450 mg once daily
200-mg dose, 1 vial for 100-mg on day 1 and 2 (as loading dose). Main-
dose). • Reconstitute each 100 mg vial tenance: 300 mg once daily for 7–14
with 5 mL Sterile Water for injection, 0.9% days.
NaCl, or 5% Dextrose injection. • Gently
swirl vial until completely dissolved. Do Dosage in Renal Impairment
not shake or agitate. • Allow vial to Mild to severe impairment: No dose
stand until foam disperses. • Visually adjustment.
inspect for particulate matter or discolor-
Dosage in Hepatic Impairment
ation. Solution should appear yellow to
Mild to severe impairment: No dose
dark orange in color. Do not use if solu-
adjustment.
tion is discolored. • Dilute in 100-mL
infusion bag containing 0.9% NaCl or 5% SIDE EFFECTS
Dextrose Injection for a final concentra-
Frequent (21%): Nausea. Occasional
tion of 1 mg/mL or 2 mg/mL.
(11%–5%): Vomiting, infusion reactions
Infusion guidelines • Infuse via dedi-
(extravasation, pain, erythema, inflam-
cated IV line or a Y-site. • Flush infu-
mation, swelling, irritation, peripheral
sion line with 0.9% NaCl or 5% Dextrose
swelling and induration). Rare (3%–
Injection before and after administration
less than 2%): Headache, diarrhea,
if infusion line is used for sequential infu-
vertigo, tachycardia, abdominal pain,
sions of several drugs.
dyspepsia, fatigue, oral pharyngeal
Rate of administration • Infuse
pain, pruritus, erythema, hyperhidro-
200-mg dose over 60 min or 100-mg
sis, urticaria.
dose over 30 min.

Canadian trade name Non-Crushable Drug High Alert drug


868 omalizumab

ADVERSE EFFECTS/TOXIC levels, protein intake. Due to prolonging


REACTIONS effect of prothrombin activity, dosage of
Serious hypersensitivity reactions, anticoagulants may need to adjusted and
including anaphylaxis, may occurred. monitored.
Tooth discoloration and enamel hypopla- PATIENT/FAMILY TEACHING
sia may occur when given during tooth
• It is essential to complete drug ther-
development (second or third trimester,
apy despite improvement of symptoms.
infancy, childhood up to 8 yrs of age).
Early discontinuation may result in anti-
May inhibit bone growth when given in
bacterial resistance or increase the risk
second or third trimester, infancy, and
of recurrent infection. • Frequent diar-
childhood up to 8 yrs of age. Clostrid-
rhea, fever, abdominal pain, blood-
ium difficile-associated diarrhea, with
streaked stool may indicate infectious
severity ranging from mild diarrhea to
diarrhea and may be contagious to oth-
fatal colitis, was reported. C. difficile
ers. • Severe allergic reactions such as
infection may occur more than 2 mos
dizziness, hives, palpitations, rash, short-
after discontinuation. May increase risk
ness of breath, tongue-swelling may oc-
of development of drug-resistant bacte-
cur. • Nausea is a common side ef-
ria or superinfection when used in the
fect. • Persistent, severe abdominal
absence of a proven or strongly sus-
pain that radiates to the back (with or
pected bacterial infection. Other adverse
without vomiting) may indicate acute in-
reactions such as acidosis, atrial fibril-
flammation of the pancreas. • Take on
lation, azotemia, hyperphosphatemia,
an empty stomach. Fasting is recom-
mycotic infections, pancreatitis, pan-
mended for 4 hrs before and 2 hrs after
creatic necrosis, pleural effusion, oral
taking tablet. Do not take antacids, mul-
candidiasis, transaminitis, elevated BUN
O tivitamins, dairy products for at least 4
have occurred with other tetracyclines
hrs after taking tablet. • Avoid preg-
and may occur with omadacycline.
nancy; may cause fetal harm. Female pts
NURSING CONSIDERATIONS of reproductive potential should use ef-
fective contraception during treatment.
BASELINE ASSESSMENT Do not breastfeed.
Question history of hypersensitivity to tet-
racycline, sulfites; predisposition to can-
didiasis infection; pancreatitis. Question
pt’s usual stool characteristics (color, omalizumab
frequency, consistency). Confirm compli-
ance of effective contraception. Receive oh-ma-liz-ue-mab
full medication history and screen for (Xolair)
interactions. j BLACK BOX ALERT jAna-
phylaxis (severe bronchospasm,
INTERVENTION/EVALUATION hypotension, angioedema, syncope,
Monitor for hypersensitivity reactions, urticaria) has occurred after first
anaphylaxis (dyspnea, hypotension, dose and in some cases after 1 yr of
regular treatment.
rash, angioedema, tachycardia). Moni- Do not confuse omalizumab
tor daily pattern of bowel activity, stool with ofatumumab.
consistency (increased severity may
indicate antibiotic-associated colitis). uCLASSIFICATION
If frequent diarrhea occurs, obtain C. PHARMACOTHERAPEUTIC: Mono-
difficile toxin test and initiate isolation clonal antibody. CLINICAL: Antiasth-
precautions until test result is confirmed; matic.
manage proper fluid intake, electrolyte

underlined – top prescribed drug


omalizumab 869

USES ADMINISTRATION/HANDLING
Treatment of moderate to severe persis- SQ
tent asthma in adults and children 6 yrs of Reconstitution • Use only Sterile
age and older reactive to perennial aller- Water for Injection to prepare for SQ
gens and with symptoms inadequately administration. • Medication takes
controlled with inhaled corticosteroids. 15–20 min to dissolve. • Draw 1.4 mL
Chronic idiopathic urticaria in adults and Sterile Water for Injection into 3-mL
children 12 yrs and older. syringe with 1-inch, 18-gauge needle;
inject contents into powdered
PRECAUTIONS vial. • Swirl vial for approximately 1
Contraindications: Hypersensitivity to min (do not shake) and again swirl vial
omalizumab. Do not use to treat acute for 5–10 sec every 5 min until no gel-like
bronchospasm, status asthmaticus. Cau- particles appear in the solution. • Do
tions: Pts at risk for parasitic infections. not use if contents do not dissolve com-
pletely within 40 min. • Invert vial for
ACTION 15 sec (allows solution to drain toward
Selectively binds to human immuno- the stopper). • Using new 3-mL syringe
globulin E (IgE). Inhibits binding of with 1-inch 18-gauge needle, obtain
IgE on surface of mast cells, basophils. required 1.2-mL dose, replace 18-gauge
Therapeutic Effect: Prevents/reduces needle with 25-gauge needle for SQ
number of asthmatic attacks and cortico- administration.
steroid use. Rate of administration • SQ admin-
istration may take 5–10 sec to administer
PHARMACOKINETICS due to its viscosity.
Absorbed slowly after SQ administration, Storage • Use only clear or slightly
with peak concentration in 7–8 days. opalescent solution; solution is slightly O
Excreted primarily via hepatic degrada- viscous. • Refrigerate. • Reconsti-
tion. Half-life: 26 days. tuted solution is stable for 8 hrs if refrig-
erated or within 4 hrs of reconstitution
LIFESPAN CONSIDERATIONS when stored at room temperature.
Pregnancy/Lactation: Because IgE
is present in breast milk, omalizumab INDICATIONS/ROUTES/DOSAGE
is expected to be present in breast b ALERT c Give only under direct
milk. Use only if clearly needed. Chil- medical supervision. Should be adminis-
dren: Safety and efficacy not established tered in health care setting by health
in pts younger than 6 yrs. Elderly: No professionals. Dosage and frequency of
age-related precautions noted. administration are based upon total IgE
levels and body weight (see table). IgE
INTERACTIONS levels should be measured prior to initi-
DRUG: May enhance the adverse/ ating treatment and not during treat-
toxic effects of belimumab, loxap- ment. Pts should be observed a mini-
ine. HERBAL: Echinacea may decrease mum of 2 hrs following each omalizumab
effects. FOOD: None known. LAB VAL- treatment.
UES: May increase serum IgE levels.
Asthma
AVAILABILITY (Rx) SQ: ADULTS, ELDERLY, CHILDREN 6 YRS
Injection, Prefilled Syringe: 75 mg/0.5 AND OLDER: 75–375 mg every 2 or 4
mL, 150 mg/mL. Injection, Powder for wks; dose and dosing frequency are
Reconstitution: 150 mg/1.2 mL after individualized based on body weight
reconstitution. and pretreatment IgE level (as shown

Canadian trade name Non-Crushable Drug High Alert drug


870 ombitasvir/­paritaprevir/ritonavir/­dasabuvir
in table). (Consult specific product Dosing not dependent on IgE level or
labeling.) body weight.
Chronic Idiopathic Urticaria Dosage in Renal/Hepatic Impairment
SQ: ADULTS, CHILDREN 12 YRS AND No dose adjustment.
OLDER: 150 mg or 300 mg q4wks.

4-Wk Dosing Table


Pretreatment Serum Weight Weight Weight Weight
IgE Levels (units/mL) 30–60 kg 61–70 kg 71–90 kg 91–150 kg
30–100 150 mg 150 mg 150 mg 300 mg
101–200 300 mg 300 mg 300 mg See next table
201–300 300 mg See next table See next table See next table

2-Wk Dosing Table


Pretreatment
Serum IgE Levels Weight Weight Weight Weight
(units/mL) 30–60 kg 61–70 kg 71–90 kg 91–150 kg
101–200 See preceding See preceding See preceding 225 mg
table table table
201–300 See preceding 225 mg 225 mg 300 mg
table
301–400 225 mg 225 mg 300 mg Do not dose
401–500 300 mg 300 mg 375 mg Do not dose
501–600 300 mg 375 mg Do not dose Do not dose
601–700 375 mg Do not dose Do not dose Do not dose
O

SIDE EFFECTS INTERVENTION/EVALUATION


Frequent (45%–11%): Injection site ecchy- Monitor rate, depth, rhythm, type of res-
mosis, redness, warmth, stinging, urticaria, pirations, quality/rate of pulse. Assess
viral infection, sinusitis, headache, pharyn- lung sounds for rhonchi, wheezing, rales.
gitis. Occasional (8%–3%): Arthralgia, leg Observe lips, fingernails for cyanosis.
pain, fatigue, dizziness. Rare (2%): Arm PATIENT/FAMILY TEACHING
pain, earache, dermatitis, pruritus.
• Increase fluid intake (decreases viscosity
ADVERSE EFFECTS/TOXIC of pulmonary secretions). • Do not alter/
REACTIONS stop other asthma medications. • Report
Anaphylaxis, occurring within 2 hrs of allergic reactions (e.g., breathing difficulty,
first dose or subsequent doses, occurs in swelling of throat/tongue).
0.1% of pts. Malignant neoplasms occur
in 0.5% of pts.
ombitasvir/­
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
paritaprevir/
Obtain baseline serum total IgE level ritonavir/­dasabuvir
before initiation of treatment (dosage is
based on pretreatment levels). Drug is om-bit-as-vir/par-i-ta-pre-vir/rit-
not for treatment of acute exacerbations oh-na-vir/da-sa-bue-vir
of asthma, acute bronchospasm, status (Viekira Pak, Holkira PAK ,
asthmaticus. Viekira XR)

underlined – top prescribed drug


ombitasvir/­paritaprevir/ritonavir/­dasabuvir 871
Test all pts for hepatitis B virus estradiol–containing drugs including
(HBV) infection prior to initiation. combined oral contraceptives, gemfi-
HBV reactivation was reported in brozil, lovastatin, lurasidone, midazolam
HBV/HCV co-infected pts who were (oral), phenytoin, PHENobarbital, pimo-
undergoing or had completed treat- zide, ranolazine, rifAMPin, sildenafil
ment with hepatitis C virus (HCV) (when used for pulmonary arterial hyper-
direct-acting antivirals and were not tension), simvastatin, St. John’s wort,
receiving HBV antiviral therapy. HBV triazolam. Cautions: History of anemia,
reactivation may cause fulminant hepatitis B virus infection, HIV infection.
hepatitis, hepatic failure, and death.
Monitor HCV/HBV co-infected pts for ACTION
hepatitis flare or HBV reactivation Ombitasvir inhibits HCV NS5A needed
during HCV infection and as clini- for essential RNA replication and virion
cally indicated. assembly. Paritaprevir inhibits HCV prote-
Do not confuse ombitasvir with ase needed for cleavage of HCV-encoded
daclatasvir, or paritaprevir with polyproteins and viral replication. Rito-
boceprevir or simeprevir, or navir inhibits CYP3A clearance; increases
ritonavir with Retrovir, lopina- plasma concentrations of paritaprevir. Das-
vir, darunavir, or saquinavir, or abuvir inhibits HCV RNA-dependent RNA
dasabuvir with sofosbuvir. polymerase needed for replication of viral
genome. Therapeutic Effect: Inhibits
uCLASSIFICATION viral replication of hepatitis C virus.
PHARMACOTHERAPEUTIC: NS5A
inhibitor, protease inhibitor, CYP3A PHARMACOKINETICS
inhibitor, nonnucleoside inhibitor. Readily absorbed. Paritaprevir, ritonavir,
CLINICAL: Antihepaciviral. dasabuvir metabolized in liver. Ombitasvir O
metabolized by amide hydrolysis. Protein
binding: ombitasvir: greater than 99%,
USES paritaprevir: 97%–99%, ritonavir: 99%,
Treatment of adults with chronic hepati- dasabuvir: 99%. Peak plasma concentra-
tis C virus (HCV) infection genotype 1a tion: 4–5 hrs. Steady-state concentra-
without cirrhosis or with compensated tion: 12 days. Elimination: ombitasvir:
cirrhosis (in combination with ribavi- feces (92%), urine (2%); paritaprevir:
rin), and genotype 1b without cirrhosis feces (88%), urine (9%); ritonavir: feces
or with compensated cirrhosis. (86%), urine (11%); dasabuvir: feces
(94%), urine (2%). Half-life: Ombitas-
PRECAUTIONS vir: 21–25 hrs; paritaprevir: 5.5 hrs; rito-
Contraindications: Hypersensitivity to any navir: 4 hrs; dasabuvir: 5.5–6 hrs.
component. Moderate to severe hepatic
impairment; decompensated hepatic cir- LIFESPAN CONSIDERATIONS
rhosis; contraindication or known hyper- Pregnancy/Lactation: Avoid pregnancy;
sensitivity to ribavirin; concomitant use of may cause fetal harm. When administered
strong CYP3A inducers, strong CYP2C8 with ribavirin, therapy is contraindicated
inducers or strong CYP2C8 inhibitors; in pregnant women and in men whose
drugs highly dependent on CYP3A for female partners are pregnant. Unknown
clearance and for which elevated plasma if distributed in breast milk. Concomitant
concentrations are associated with seri- use of ethinyl estradiol–containing drugs is
ous and/or life-threatening events. Con- contraindicated. Alternative contraception
current use of alfuzosin, carBAMazepine, methods including progestin-only drugs,
colchicine, dronedarone, efavirenz, barrier methods, abstinence are recom-
ergotamine, dihydroergotamine, ethinyl mended. Children: Safety and efficacy not

Canadian trade name Non-Crushable Drug High Alert drug


872 ombitasvir/­paritaprevir/ritonavir/­dasabuvir
established. Elderly: No age-related pre- twice daily with or without ribavirin.
cautions noted. (Viekira XR): 3 tablets once daily.

INTERACTIONS Treatment Regimen and Duration


DRUG: May increase concentration/ Genotype 1a, without cirrhosis
effects of antiarrhythmics (e.g., amio- (in combination with ribavirin);
darone), antifungals (e.g., itracon- genotype 1b without cirrhosis or
azole), calcium channel blockers compensated cirrhosis: Fixed-com-
(e.g., amLODIPine, NIFEdipine), bination regimen with ribavirin for 12
corticosteroids (e.g., fluticasone), wks. Recommended dose of ribavi-
immunosuppressants (e.g., cyclo- rin based on weight in kg: LESS THAN
SPORINE), digoxin, HIV antiretrovi- 75 KG: 1,000 mg/day in 2 divided doses.
rals (e.g., paritaprevir, rilpivirine), 75 KG OR GREATER: 1,200 mg/day in 2
phosphodiesterase-5 inhibitors divided doses. For ribavirin dose modifi-
(e.g., sildenafil), sedative/hypnot- cations, refer to prescribing information.
ics (e.g., temazepam), statins (e.g.,
Dose Modification
atorvastatin, simvastatin), siroli-
Liver Transplant Recipients
mus, tacrolimus. Anticonvulsants
PO: ADULTS, ELDERLY: 2 tablets of ombi-
(e.g., carBAMazepine, phenytoin),
dexamethasone, efavirenz, omepra- tasvir, paritaprevir, ritonavir once daily,
zole, rifAMPin may decrease concen- plus 1 tablet of dasabuvir twice daily with
tration/effect. HERBAL: St. John’s wort ribavirin for 24 wks, irrespective of HCV
may decrease concentration/effect. Kava genotype 1 subtype in pts with normal
kava may increase risk of hepatotoxicity. hepatic function and mild fibrosis.
HCV/HIV-1 Coinfection
Red yeast may increase risk of myopa-
O thy, rhabdomyolysis. Meals increase Follow dose recommendations as listed
absorption. FOOD: Grapefruit prod- in Treatment Regimen and Duration.
ucts, Seville oranges may increase Consider suppressive antiretroviral drug
concentration/effect. LAB VALUES: May therapy during treatment.
increase serum alkaline phosphatase, Dosage in Renal Impairment
ALT, INR. May decrease Hct, Hgb. No dose adjustment.
AVAILABILITY (Rx) Dosage in Hepatic Impairment
Fixed-Dose Combination Tablets (co- Mild impairment: No dose adjustment.
packaged with dasabuvir tablets): (Viekira Moderate impairment: Treatment
Pak): Ombitasvir 12.5 mg/paritaprevir not recommended. Severe impair-
75 mg/ritonavir 50 mg; dasabuvir 250 mg. ment: Treatment contraindicated.
(Viekira XR): Ombitasvir 8.33 mg/parita-
previr 50 mg/ritonavir 33.3 mg/dasabu- SIDE EFFECTS
vir 200 mg. Frequent (34%–22%): Fatigue, nausea.
Occasional (18%–14%): Pruritus, rash,
ADMINISTRATION/HANDLING erythema, eczema, allergic dermatitis,
PO skin exfoliation, urticaria, photosen-
• Give with food. Do not cut, crush, sitivity reaction, skin ulcer, insomnia,
break, or divide XR tablets. asthenia.
INDICATIONS/ROUTES/DOSAGE ADVERSE EFFECTS/TOXIC
Hepatitis C Virus Infection REACTIONS
PO: ADULTS, ELDERLY: (Viekira Pak): 2 HBV reactivation was reported in pts co-
tablets of ombitasvir, paritaprevir, ritona- infected with HBV/HVC; may result in ful-
vir once daily, plus 1 tablet of dasabuvir minant hepatitis, hepatic failure, death.
underlined – top prescribed drug
omega-3 acid-ethyl esters 873
Serum ALT greater than 5 times upper unless approved by doctor who originally
limit of normal (ULN) reported in 1% of started treatment. Do not take herbal
pts (usually occurred during the first 4 products. • Pregnancy should be
wks of treatment). Elevations of serum avoided when combination regimen is
ALT were significantly higher in female pts given with ribavirin. Female pts of child-
using ethinyl estradiol–containing drugs bearing potential must use reliable forms
such as contraceptive patches, combined of birth control such as progestin-­
oral contraceptives, vaginal rings. May containing contraception, barrier
increase risk of drug resistance in HCV/ ­methods, abstinence. Immediately report
HIV-1 coinfected pts using HIV-1 prote- suspected pregnancy. Do not breast-
ase inhibitors. Hypersensitivity reaction feed. • Report abdominal pain, bruis-
including angioedema may occur. ing easily, dark-colored urine, fatigue,
yellowing of the skin or eyes. • Avoid
NURSING CONSIDERATIONS alcohol. • Report skin changes such as
BASELINE ASSESSMENT rash, peeling, ulcers; allergic reactions
such as difficulty breathing, itching,
Obtain baseline CBC, LFT, HCV-RNA level, hives, tongue swelling.
urine pregnancy. Confirm HCV genotype.
Test all pts for hepatitis B virus (HBV)
infection prior to initiation. Receive full
medication history and screen for con- omega-3 acid-
traindications/interactions. Ethinyl es-
tradiol–containing contraceptive drugs ethyl esters
should be discontinued prior to initiation.
Question history as listed in Precautions. oh-may-ga 3 as-id eth-il es-ters
To reduce risk of HIV-1 protease inhibitor (Lovaza, Vascepa)
Do not confuse Lovaza with O
drug resistance, consider suppressive an-
tiretroviral drug therapy upon initiation. LORazepam.
INTERVENTION/EVALUATION uCLASSIFICATION
Monitor LFT periodically during the first PHARMACOTHERAPEUTIC: Omega-3
4 wks of treatment, then as clinically in- fatty acid. CLINICAL: Antilipemic
dicated thereafter. Discontinue treatment agent.
for serum ALT persistently greater than 10
times ULN; serum ALT elevation associated
with increase in serum alkaline phospha- USES
tase, bilirubin, or INR; hepatic injury. Adjunct to diet to reduce very high (500
Periodically monitor CBC for anemia, mg/dL or higher) serum triglyceride lev-
HCV-RNA level for treatment effective- els in adult pts. Dietary supplement for
ness. Reinforce birth control compliance. pts with early risk of CAD. OFF-LABEL:
Monitor for abdominal pain, bruising, Treatment of IgA nephropathy.
jaundice, nausea, vomiting; may indicate
hepatic injury. Ethinyl estradiol–contain- PRECAUTIONS
ing contraceptives may be restarted ap- Contraindications: Hypersensitivity to
prox. 2 wks after discontinuation. omega-3 fatty acids. Cautions: Known
sensitivity, allergy to fish.
PATIENT/FAMILY TEACHING
• Treatment must be used in combina- ACTION
tion with ribavirin. • Take with Reduces hepatic production of triglyceride­-
meals. • Inform pt of contraindica- rich very low density lipoproteins (VLDL).
tions/adverse effects of therapy. • Do Therapeutic Effect: Reduces serum tri-
not take newly prescribed medication glyceride levels.
Canadian trade name Non-Crushable Drug High Alert drug
874 omeprazole

PHARMACOKINETICS ADVERSE EFFECTS/TOXIC


Well absorbed following PO administra- REACTIONS
tion. Incorporated into phospholipids. None known.
Half-life: N/A.
NURSING CONSIDERATIONS
LIFESPAN CONSIDERATIONS BASELINE ASSESSMENT
Pregnancy/Lactation: Unknown Assess baseline serum triglyceride level,
if distributed in breast milk. Chil- LFT. Obtain diet history, esp. fat con-
dren: Safety and efficacy not established sumption.
in pts younger than 18 yrs. Elderly: No
age-related precautions noted. INTERVENTION/EVALUATION
Monitor serum triglyceride levels for
INTERACTIONS therapeutic response. Monitor serum
DRUG: May increase antiplatelet effect ALT, LDL periodically during therapy. Dis-
of agents with antiplatelet proper- continue therapy if no response after 2
ties (e.g., NSAIDS, aspirin). May mos of treatment.
increase anticoagulant effect of anti- PATIENT/FAMILY TEACHING
coagulants (e.g., warfarin). HERBAL:
None significant. FOOD: None known. • Continue to adhere to lipid-lowering
LAB VALUES: May increase serum ALT, diet (important part of treatment). • Pe-
LDL. riodic lab tests are essential part of ther-
apy to determine drug effectiveness.
AVAILABILITY (Rx)
Capsules: 500 mg, 1,000 mg.
O
ADMINISTRATION/HANDLING omeprazole
PO
• Give without regard to food. oh-mep-ra-zole
(Losec , PriLOSEC, PriLOSEC
INDICATIONS/ROUTES/DOSAGE OTC)
Do not confuse omeprazole with
b ALERT c Before initiating therapy, pt
ARIPiprazole, pantoprazole,
should be on standard cholesterol-­ or esomeprazole, or PriLOSEC
lowering diet for minimum of 3–6 mos. with Plendil, Prevacid, Prinivil,
Continue diet throughout therapy. or PROzac.
Usual Dosage
FIXED-COMBINATION(S)
PO: ADULTS, ELDERLY: (Lovaza): 4 g (4
capsules) once daily or 2 g (2 capsules) Yosprala: omeprazole/aspirin (a
twice daily. (Vascepa): 2 g (2 [1 gram] platelet aggregation inhibitor): 40
capsules or 4 [0.5 g] capsules) twice mg/81 mg, 40 mg/325 mg. Zegerid:
daily with meals. 4 g/day, given as a single omeprazole/sodium bicarbonate
daily dose or twice daily. (an antacid): 20 mg/1,100 mg, 40
mg/1,100 mg. Zegerid Powder: 20
Dosage in Renal/Hepatic Impairment mg/1,680 mg, 40 mg/1,680 mg.
No dose adjustment.
uCLASSIFICATION
SIDE EFFECTS PHARMACOTHERAPEUTIC: Benzi-
Occasional (5%–3%): Eructation, altered midazole. CLINICAL: Proton pump
taste, dyspepsia. Rare (2%–1%): Rash, inhibitor.
back pain.
underlined – top prescribed drug
omeprazole 875

USES INTERACTIONS
Short-term treatment (4–8 wks) of ero- DRUG: May decrease concentration/
sive esophagitis (diagnosed by endos- effects of acalabrutinib, atazanavir,
copy), symptomatic gastroesophageal bosutinib, cefuroxime, clopidogrel,
reflux disease (GERD) poorly responsive dasatinib, neratinib. May increase
to other treatment. H. pylori–associated concentration/effects of escitalopram,
duodenal ulcer (with amoxicillin and voriconazole, oral anticoagu-
clarithromycin). Long-term treatment of lants (e.g., warfarin), phenytoin.
pathologic hypersecretory conditions, HERBAL: St. John’s wort may decrease
treatment of active duodenal ulcer or concentration/effects. FOOD: None
active benign gastric ulcer. Maintenance known. LAB VALUES: May increase
healing of erosive esophagitis. OTC, serum alkaline phosphatase, ALT, AST.
short-term: Treatment of frequent,
uncomplicated heartburn occurring 2 or AVAILABILITY (Rx)
more days/wk. OFF-LABEL: Prevention/ Oral Suspension: 2.5 mg/packet, 10 mg/
treatment of NSAID-induced ulcers, stress packet.
ulcer prophylaxis in critically ill pts. Capsules, Delayed-Release: (PriLO-
SEC): 10 mg, 20 mg, 40 mg. Tablets,
PRECAUTIONS Delayed-Release: (PriLOSEC OTC): 20 mg.
Contraindications: Hypersensitivity to
omeprazole, other proton pump inhibitors. ADMINISTRATION/HANDLING
Concomitant use with products containing PO
rilpivirine. Cautions: May increase risk • Give before meals (breakfast pre-
of fractures, gastrointestinal infections. ferred). • Give whole. Do not break,
Hepatic impairment, pts of Asian descent. crush, dissolve, or divide delayed-release O
forms. • May open capsule, mix with
ACTION applesauce, and give immediately.
Inhibits hydrogen-potassium adenosine
triphosphatase (H+/K+ ATP pump), an PO (Suspension)
enzyme on the surface of gastric parietal • Following reconstitution, allow to
cells. Therapeutic Effect: Increases thicken (2–3 min). • Administer
gastric pH, reduces gastric acid within 30 min.
production.
INDICATIONS/ROUTES/DOSAGE
PHARMACOKINETICS Active Duodenal Ulcer
Route Onset Peak Duration PO: ADULTS, ELDERLY: 20–40 mg once
PO 1 hr 2 hrs 72 hrs daily for 4 wks.
Rapidly absorbed from GI tract. Protein Symptomatic GERD
binding: 95%. Primarily distributed into PO: ADULTS, ELDERLY, CHILDREN WEIGH-
gastric parietal cells. Metabolized in liver. ING 20 KG OR MORE: 10 mg once daily. May
Primarily excreted in urine. Unknown if increase to 20 mg once daily after 4–8 wks
removed by hemodialysis. Half-life: 0.5–1 if necessary. Discontinue once asymptom-
hr (increased in hepatic impairment). atic for 8 wks. 10–19 KG: 10 mg/day for up
to 4 wks. 5–9 KG: 5 mg/day for up to 4 wks.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if Erosive Esophagitis
drug crosses placenta or is distributed in PO: ADULTS, ELDERLY, CHILDREN WEIGH-
breast milk. Children: Safety and efficacy ING 20 KG OR MORE: Treatment: 20–40 mg
not established. Elderly: Use caution once daily. Once symptoms are controlled,
(bioavailability may be increased). continue for at least 8 wks. CHILDREN

Canadian trade name Non-Crushable Drug High Alert drug


876 ondansetron
1–16 YRS WEIGHING 10–19 KG: 10 mg/day. PATIENT/FAMILY TEACHING
WEIGHING 5–9 KG: 5 mg/day. CHILDREN 1–11 • Report headache, onset of black, tarry
MOS WEIGHING 10 KG OR MORE: 10 mg/ stools, diarrhea, abdominal pain.
day. WEIGHING 5–9 KG: 5 mg/day. WEIGH- • Avoid alcohol. • Swallow capsules
ING 3–4 KG: 2.5 mg/day. Maintenance: whole; do not chew, crush, dissolve, or
ADULTS, ELDERLY, CHILDREN WEIGHING 20 divide. • Take before eating.
KG OR MORE: 20 mg/day for up to 12 mos
(including treatment period). ASIAN PTS,
CHILDREN WEIGHING 10–19 KG: 10 mg/day.
WEIGHING 5–9 KG: 5 mg/day. ondansetron
Pathologic Hypersecretory Conditions on-dan-se-tron
Note: Doses more than 80 mg in divided (Zofran, Zuplenz)
doses. PO: ADULTS, ELDERLY: Initially, 40 Do not confuse ondansetron
mg twice daily. May titrate up to 180 mg/day. with dolasetron, granisetron,
H. Pylori Duodenal Ulcer
or palonosetron, or Zofran with
PO: ADULTS, ELDERLY: 20 mg or 40 mg Zantac or Zosyn.
twice daily as part of an appropriate com- uCLASSIFICATION
bination regimen with antibiotics (dose
depends on the selected regimen). PHARMACOTHERAPEUTIC: Selective
5-HT3 receptor antagonist. CLINI-
Gastric Ulcer CAL: Antinausea, antiemetic.
PO: ADULTS, ELDERLY: 20–40 mg once
daily for 8 wks.
USES
O OTC Use (Frequent Heartburn) Prevention/treatment of nausea/vomiting
PO: ADULTS, ELDERLY: 20 mg/day for 14 due to cancer chemotherapy (includ-
days. May repeat after 4 mos if needed. ing high-dose CISplatin). Prevention and
treatment of postop nausea, vomiting. Pre-
Dosage in Renal/Hepatic Impairment vention of radiation-induced nausea, vom-
No dose adjustment. iting. OFF-LABEL: Breakthrough treatment
of nausea and vomiting associated with
SIDE EFFECTS chemotherapy, hyperemesis gravidarum.
Frequent (7%): Headache. Occasional
(3%–2%): Diarrhea, abdominal pain, PRECAUTIONS
nausea. Rare (2%): Dizziness, asthenia, Contraindications:Hypersensitivity to
vomiting, constipation, upper respiratory ondansetron, other HT3 antagonists.
tract infection, back pain, rash, cough. Concomitant use of apomorphine. Cau-
tions: Mild to moderate hepatic impair-
ADVERSE EFFECTS/TOXIC ment, pts at risk for QT prolongation
REACTIONS or ventricular arrhythmia (congenital
Pancreatitis, hepatotoxicity, interstitial long QT prolongation, medications
nephritis occur rarely. May increase risk prolonging QT interval, hypokalemia,
of C. difficile infection. hypomagnesemia).
NURSING CONSIDERATIONS ACTION
INTERVENTION/EVALUATION
Blocks serotonin, both peripherally on
vagal nerve terminals and centrally in
Evaluate for therapeutic response (relief chemoreceptor trigger zone. Therapeu-
of GI symptoms). Question if GI discom- tic Effect: Prevents nausea/vomiting.
fort, nausea, diarrhea occurs.

underlined – top prescribed drug


ondansetron 877

PHARMACOKINETICS PO
Readily absorbed from GI tract. Pro- • Give without regard to food.
tein binding: 70%–76%. Metabolized Orally Disintegrating Tablets
in liver. Primarily excreted in urine. • Do not remove from blister pack until
Unknown if removed by hemodialysis. needed. • Peel backing off; do not push
Half-life: 3–6 hrs (increased in hepatic through. • Place tablet on tongue;
impairment). allow to dissolve. • Swallow with saliva.
LIFESPAN CONSIDERATIONS Oral Soluble Film
Pregnancy/Lactation: Unknown if • Keep film in pouch until ready to
drug crosses placenta or is distributed use. • Remove film strip from pouch and
in breast milk. Children: Safety and effi- place on top of tongue; allow to dis-
cacy not established in children younger solve. • Swallow after film dissolves. Do
than 1 mo. Elderly: No age-related pre- not chew or swallow film whole. • If using
cautions noted. more than one, each should be allowed to
dissolve before administering the next one.
INTERACTIONS
DRUG: Apomorphine may cause pro- IV INCOMPATIBILITIES
found hypotension, altered LOC. QT Acyclovir (Zovirax), allopurinol (Aloprim),
interval–prolonging medications amphotericin B (Fungizone), ampho-
(e.g., amiodarone, azithromycin, cip- tericin B complex (Abelcet, AmBisome,
rofloxacin, haloperidol) may increase Amphotec), ampicillin (Polycillin), ampi-
risk of QT interval prolongation, torsades cillin and sulbactam (Unasyn), cefepime
de pointes. HERBAL: St. John’s wort (Maxipime), 5-­fluorouracil, LORazepam
may decrease concentration. FOOD: None (Ativan), meropenem (Merrem IV), methyl-
known. LAB VALUES: May transiently O
PREDNISolone (SOLU-Medrol).
increase serum bilirubin, ALT, AST.
IV COMPATIBILITIES
AVAILABILITY (Rx) CARBOplatin (Paraplatin), CISplatin
Injection Solution: (Zofran): 2 mg/mL. (Platinol), cyclophosphamide (Cytoxan),
Oral Soluble Film: (Zuplenz): 4 mg, 8 mg. cytarabine (Cytosar), dacarbazine (DTIC-
Oral Solution: (Zofran): 4 mg/5 mL. Tab- Dome), DAUNOrubicin (Cerubidine),
lets: (Zofran): 4 mg, 8 mg, 24 mg. Tab- dexmedetomidine (Precedex), dexameth-
lets, Orally Disintegrating: 4 mg, 8 mg. asone (Decadron), diphenhydrAMINE
(Benadryl), DOCEtaxel (Taxotere), DOPa-
ADMINISTRATION/HANDLING mine (Intropin), etoposide (VePesid),
IV gemcitabine (Gemzar), heparin, HYDRO-
morphone (Dilaudid), ifosfamide (Ifex),
Reconstitution • May give undi- magnesium, mannitol, mesna (Mesnex),
luted. • For IV infusion, dilute with 50 mL methotrexate, metoclopramide (Reglan),
D5W or 0.9% NaCl before administration. mitoMYcin (Mutamycin), mitoXANTRONE
Rate of administration • Give IV (Novantrone), morphine, PACLitaxel
push over 2–5 min. • Give IV infusion (Taxol), potassium chloride, teniposide
over 15–30 min. (Vumon), topotecan (Hycamtin), vin-
Storage • Store at room tempera- BLAStine (Velban), vinCRIStine (Onco-
ture. • Stable for 48 hrs at room tem- vin), vinorelbine (Navelbine).
perature following dilution.
INDICATIONS/ROUTES/DOSAGE
IM
Chemotherapy-Induced Nausea/Vomiting
• Inject undiluted into large muscle
IV: ADULTS, ELDERLY, CHILDREN 6 MOS AND
mass.
OLDER: 0.15 mg/kg (Maximum: 16 mg/
Canadian trade name Non-Crushable Drug High Alert drug
878 oritavancin
dose) 3 times/day beginning 30 min before pain, xerostomia, fever, feeling of cold,
chemotherapy, followed by subsequent redness/pain at injection site, paresthe-
doses 4 and 8 hrs after the first dose. sia, asthenia (loss of strength, energy).
PO: ADULTS, ELDERLY, CHILDREN 12 YRS Rare (1%): Hypersensitivity reaction
AND OLDER: (highly emetogenic) 16 mg 30 (rash, pruritus), blurred vision.
min before start of chemotherapy, (mod-
erately emetogenic) 8 mg repeat dose 8 ADVERSE EFFECTS/TOXIC
hrs after initial dose, then q12h, beginning REACTIONS
30 min before chemotherapy and continu- Hypertension, acute renal failure, GI
ing for 1–2 days after completion of che- bleeding, respiratory depression, coma,
motherapy. CHILDREN 4–11 YRS: 4 mg 30 extrapyramidal effects occur rarely. QT
min before chemotherapy, repeat 4 and 8 interval prolongation, torsades de
hrs after initial dose then q8h for 1–2 days pointes may occur.
after chemotherapy completed.
NURSING CONSIDERATIONS
Prevention of Postop Nausea/Vomiting
BASELINE ASSESSMENT
IV, IM: ADULTS, ELDERLY, CHILDREN OLDER
THAN 12 YRS: 4 mg as a single dose. CHIL- Assess degree of nausea, vomiting. As-
DREN 1 MO–12 YRS WEIGHING MORE THAN sess for dehydration if excessive vomiting
40 KG: 4 mg as a single dose. CHILDREN 1 occurs (poor skin turgor, dry mucous
MO–12 YRS WEIGHING 40 KG OR LESS: 0.1 membranes, longitudinal furrows in
mg/kg as a single dose. tongue). Provide emotional support.
PO: ADULTS, ELDERLY: 16 mg 1 hr INTERVENTION/EVALUATION
before induction of anesthesia.
Monitor ECG in pts with electrolyte abnor-
Prevention of Radiation-Induced Nausea/ malities (e.g., hypokalemia, hypomagne-
O semia), HF, bradyarrhythmias, concur-
Vomiting
PO: ADULTS, ELDERLY:(Total body irradi- rent use of other medications that may
ation): 8 mg 1–2 hrs before each fraction cause QT prolongation, pts receiving high
of radiotherapy administered each day. doses or frequent doses. Provide support-
(Single high-dose radiotherapy to abdo- ive measures. Assess mental status. Assess
men): 8 mg 1–2 hrs before irradiation, bowel sounds for peristalsis. Monitor
then 8 mg q8h after first dose for 1–2 daily pattern of bowel activity, stool con-
days after completion of radiotherapy. sistency. Record time of evacuation.
(Daily fractionated radiotherapy to abdo- PATIENT/FAMILY TEACHING
men): 8 mg 1–2 hrs before irradiation,
then 8 mg 8 hrs after first dose for each • Relief from nausea/vomiting generally
day of radiotherapy. occurs shortly after drug administra-
tion. • Avoid alcohol, barbiturates. •
Dosage in Renal Impairment Report persistent vomiting. • Avoid tasks
No dose adjustment. that require alertness, motor skills until
response to drug is established (may cause
Dosage in Hepatic Impairment drowsiness, dizziness).
Mild to moderate impairment: No
dose adjustment. Severe impair-
ment: Maximum daily dose: 8 mg.
oritavancin
SIDE EFFECTS
Frequent (13%–5%): Anxiety, dizziness, or-it-a-van-sin
drowsiness, headache, fatigue, constipa- (Orbactiv)
tion, diarrhea, hypoxia, urinary reten- Do not confuse oritavancin with
tion. Occasional (4%–2%): Abdominal dalbavancin or telavancin.
underlined – top prescribed drug
oritavancin 879
uCLASSIFICATION INTERACTIONS
PHARMACOTHERAPEUTIC: Lipo- DRUG: May decrease therapeutic effect of
glycopeptide (antibacterial). CLINI- anticoagulants (e.g., heparin, war-
CAL: Antibiotic. farin). Use of heparin within 48 hrs of
dose contraindicated. May increase risk of
bleeding with warfarin. HERBAL: None
USES significant. FOOD: None known. LAB
Treatment of adult pts with acute bacte- VALUES: May prolong aPTT (falsely
rial skin and skin structure infections elevates aPTT for up to 120 hrs after ori-
(ABSSSI) caused by susceptible strains tavancin administration), PT/INR. May
of gram-positive microorganisms includ- increase ALT, AST, bilirubin, uric acid. May
ing Staphylococcus aureus (including decrease glucose.
methicillin-susceptible and methicillin-
resistant strains), Streptococcus aga- AVAILABILITY (Rx)
lactiae, Streptococcus dysgalactiae, Sterile Powder for Injection: 400 mg/vial.
Streptococcus pyogenes, Streptococcus
anginosus group (including S. angino- ADMINISTRATION/HANDLING
sus, S. intermedius, S. constellatus), IV
and E. faecalis (vancomycin-susceptible
strains only). b ALERT c No preservatives or bacte-
riostatic agent is present in product.
PRECAUTIONS Aseptic technique must be used when
Contraindications: Hypersensitivity preparing solution. Must be reconsti-
to oritavancin. Concomitant use of IV tuted with Sterile Water for Injection and
unfractionated heparin sodium for 120 subsequently diluted with 5% Dextrose in
hrs (5 days) after oritavancin adminis- Water only. O
tration. Cautions: Severe hepatic impair- Reconstitution • Obtain three 400-
ment, history of hypersensitivity reaction mg vials to equal required 1,200-mg
to glycopeptides (e.g., vancomycin), dose. • Add 40 mL of Sterile Water for
recent C. difficile infection or antibiotic- Injection to each vial for final concentra-
associated colitis. tion of 10 mg/mL per vial. • To avoid
foaming, gently swirl until contents com-
ACTION pletely dissolve. • Visually inspect
Inhibits cell wall synthesis by binding each vial for particulate matter or
to bacterial cell membrane, disrupt- discoloration.
ing membrane integrity. Therapeutic Dilution • Using D5W, withdraw 120 mL
Effect: Bactericidal. from 1,000-mL bag and discard.
• Withdraw 40 mL from each vial and mix
PHARMACOKINETICS into D5W to provide a final concentration
Widely distributed. Not metabolized. Pro- of 1.2 mg/mL.
tein binding: 85%. Excreted unchanged Rate of administration • Administer
in feces, urine. Not removed by hemodi- over 3 hrs.
alysis. Half-life: 10.2 days. Storage • Reconstituted solution
should appear clear, colorless to pale
LIFESPAN CONSIDERATIONS yellow. • Infuse diluted solution within
Pregnancy/Lactation: Unknown if dis- 6 hrs when stored at room temperature
tributed in breast milk. Children: Safety or 12 hrs when refrigerated. • Com-
and efficacy not established. Elderly: No bined storage time and 3-hr infusion
age-related precautions noted. time should not exceed 6 hrs if at room
temperature or 12 hrs if refrigerated.

Canadian trade name Non-Crushable Drug High Alert drug


880 oseltamivir

IV INCOMPATIBILITIES INTERVENTION/EVALUATION
Dilute using 5% Dextrose in Water only. Assess skin infection/wound for improve-
Dilution with normal saline may cause ment. Monitor daily pattern of bowel ac-
precipitate formation. Infuse via dedi- tivity, stool consistency; increasing ­severity
cated line only. Do not piggyback through of diarrhea may indicate antibiotic-as-
maintenance IV line. sociated colitis. If frequent diarrhea oc-
curs, obtain C. difficile toxin screen and
INDICATIONS/ROUTES/DOSAGE initiate isolation precautions until result
Acute Bacterial Skin and Skin Structure confirmed. Encourage PO intake. Monitor
Infection I&O. If osteomyelitis suspected, other anti-
IV: ADULTS, ELDERLY: 1,200 mg as single microbial agents may be required. Screen
dose. for hypersensitivity reaction.
PATIENT/FAMILY TEACHING
Dosage in Renal/Hepatic Impairment
Mild to moderate impairment: No • Treatment will consist of a single infu-
dose adjustment. Severe impair- sion only. • Report episodes of diarrhea,
ment: Use caution. esp. the following weeks after treatment
completion. Frequent diarrhea, fever, ab-
SIDE EFFECTS dominal pain, blood-streaked stool may
Occasional (10%–5%): Nausea, head- indicate C. difficile infection, which may
ache, vomiting. Rare (4%–3%): Diarrhea, be contagious to others. • Report ab-
dizziness, tachycardia. dominal pain, black/tarry stools, bruising,
yellowing of skin or eyes; dark urine, de-
ADVERSE EFFECTS/TOXIC creased urine output; or allergic reactions
REACTIONS including difficulty breathing, itching,
O Serious hypersensitivity reactions includ- hives, tongue swelling, wheezing. • Do
ing anaphylaxis, angioedema, broncho- not breastfeed. • Drink plenty of flu-
spasm, severe skin reactions, wheezing ids. • Report symptoms of bone pain;
have been reported with glycopeptide may indicate bone infection.
antibacterial agents. C. difficile–asso-
ciated diarrhea with severity ranging
from mild diarrhea to fatal colitis has
occurred. Treatment in the absence of oseltamivir
proven or strongly suspected bacterial
infection may increase risk of drug- oh-sel-tam-i-veer
resistant bacteria. Infusion site reactions, (Tamiflu)
phlebitis, irritation, abscess, rash, pruri- Do not confuse Tamiflu with
tus have occurred. Increased incidence Thera-flu.
of osteomyelitis has been reported.
uCLASSIFICATION
NURSING CONSIDERATIONS PHARMACOTHERAPEUTIC: Neurami-
nidase inhibitor. CLINICAL: Antiviral.
BASELINE ASSESSMENT
Obtain baseline CBC (WBC), BMP, LFT,
wound culture and sensitivity, vital signs. USES
Question history of recent C. difficile Symptomatic treatment of uncomplicated
infection, hepatic/renal impairment, acute illness caused by influenza A or B
hypersensitivity reaction. Assess skin virus in adults and children 2 wks of age
wound characteristics, hydration status. and older who are symptomatic no lon-
Question pt’s usual stool characteristics ger than 2 days. Prevention of influenza
(color, frequency, consistency). in adults, children.

underlined – top prescribed drug


oseltamivir 881

PRECAUTIONS PO: ADULTS, ELDERLY, CHILDREN 13 YRS


AND OLDER: 75 mg twice daily for 5
Contraindications: Hypersensitivity to
oseltamivir. Cautions: Renal impairment. days. CHILDREN 1–12 YRS, WEIGHING MORE
THAN 40 KG: 75 mg twice daily for 5 days.
ACTION WEIGHING 24–40 KG: 60 mg twice daily
Selective inhibitor of influenza virus neur- for 5 days. WEIGHING 16–23 KG: 45 mg
aminidase, an enzyme essential for viral twice daily for 5 days. WEIGHING 15 KG OR
LESS: 30 mg twice daily for 5 days. NEO-
replication. Acts against influenza A and B
NATES, INFANTS AGES 2 WKS TO YOUNGER
viruses. Therapeutic Effect: Suppresses
THAN 1 YR: 3 mg/kg twice daily for 5 days.
spread of infection within respiratory sys-
tem, reduces duration of clinical symptoms. Prevention of Influenza
PHARMACOKINETICS Note: Initiate within 48 hrs of contact
with an infected individual. Duration:
Readily absorbed after PO administra- 7–10 days (longer during community out-
tion. Protein binding: 3%. Metabolized in breaks). PO: ADULTS, ELDERLY, CHILDREN 13
liver. Primarily excreted in urine. Half- YRS AND OLDER: 75 mg once daily. CHILDREN
life: 6–10 hrs. 1–12 YRS, WEIGHING MORE THAN 40 KG: 75
LIFESPAN CONSIDERATIONS mg once daily. WEIGHING 24–40 KG: 60 mg
once daily. WEIGHING 15–23 KG: 45 mg once
Pregnancy/Lactation: Unknown if dis-
daily. WEIGHING LESS THAN 15 KG: 30 mg
tributed in breast milk. Children: Safety once daily. INFANTS 9–11 MOS: 3.5 mg/kg/
and efficacy not established in pts younger dose. INFANTS 3–8 MOS: 3 mg/kg/dose.
than 2 wks. Elderly: No age-related pre-
cautions noted. Dosage in Renal Impairment
CrCl 31–60 mL/min: Treatment: 30 mg
INTERACTIONS O
twice daily. Prevention: 30 mg once daily.
DRUG: Live attenuated influenza virus CrCl 11–30 mL/min: Treatment: 30 mg
vaccine intranasal may interfere with effect. once daily. Prevention: 30 mg every other
HERBAL: None significant. FOOD: None day. End-stage renal disease: Not
known. LAB VALUES: None significant. recommended.
AVAILABILITY (Rx) Dosage in Hepatic Impairment
Capsules: 30 mg, 45 mg, 75 mg. Powder No dose adjustment.
for Oral Suspension: 6 mg/mL.
SIDE EFFECTS
ADMINISTRATION/HANDLING Frequent (10%–7%): Nausea, vomiting,
PO diarrhea. Rare (2%–1%): Abdominal
• Give without regard to food. • May pain, bronchitis, dizziness, headache,
open capsules and mix with sweetened cough, insomnia, fatigue, vertigo.
liquid. • Oral suspension stable for 10 ADVERSE EFFECTS/TOXIC
days (room temperature) or 17 days REACTIONS
(refrigerated) following reconstitution.
Colitis, pneumonia, tympanic membrane
INDICATIONS/ROUTES/DOSAGE disorder, fever occur rarely.
Treatment of Influenza
NURSING CONSIDERATIONS
Note: Hospitalized pts may require lon-
ger treatment course. Initiate within 48 BASELINE ASSESSMENT
hrs of onset of symptoms. Consider dura- Obtain baseline laboratory tests as indi-
tion longer than 5 days in pts with severe cated. Confirm presence of influenza A
or complicated influenza. or B virus.

Canadian trade name Non-Crushable Drug High Alert drug


882 osimertinib
INTERVENTION/EVALUATION interval, hypokalemia, hypomagnesemia);
Monitor serum glucose, renal function history of CVA, pulmonary embolism. Con-
in pts with influenza symptoms, diabetes. comitant use of CYP3A inducers.
PATIENT/FAMILY TEACHING ACTION
• Begin as soon as possible from first Exhibits antitumor activity by irrevers-
appearance of flu symptoms (recom- ibly binding to mutant forms of EGFR.
mended within 2 days from symptom Therapeutic Effect: Inhibits tumor cell
onset). • Avoid contact with those who growth and metastasis.
are at high risk for influenza. • Not a
substitute for flu shot. PHARMACOKINETICS
Widely distributed. Metabolized in liver. Pro-
tein binding: Likely high. Peak plasma con-
centration: 3–24 hrs (median: 6 hrs). Steady
osimertinib state reached in 15 days. Excreted in feces
(68%), urine (14%). Half-life: 48 hrs.
oh-sim-er-ti-nib
(Tagrisso) LIFESPAN CONSIDERATIONS
Do not confuse osimertinib with Pregnancy/Lactation: Avoid preg-
afatinib, dasatinib, erlotinib, nancy; may cause fetal harm. Females of
ibrutinib, imatinib, olaparib, reproductive potential should use effec-
or ospemifene, or Tagrisso with tive contraception during treatment and
Targretin or Tasigna. for at least 6 wks after discontinuation.
Males with female partners of reproduc-
uCLASSIFICATION
tive potential must use effective barrier
O PHARMACOTHERAPEUTIC: Epider- methods during treatment and at least
mal growth factor receptor (EGFR) 4 mos after discontinuation. Unknown if
inhibitor. Tyrosine kinase inhibitor. distributed in breast milk. Breastfeeding
CLINICAL: Antineoplastic. not recommended during treatment and
for up to 2 wks after discontinuation. May
impair fertility in both females and males.
USES Children: Safety and efficacy not estab-
Treatment of pts with metastatic epidermal lished. Elderly: May have increased
growth factor receptor (EGFR) T790M risk of CTCAE Grade 3 or 4 adverse
mutation-positive non–small-cell lung events. May require more frequent dose
cancer (NSCLC), as detected by FDA- modifications.
approved test, who have progressed on or
after EGFR therapy. First-line treatment of INTERACTIONS
metastatic NSCLC in pts with EGFR exon 19 DRUG: QTc interval–prolonging
deletions or exon 21 L858R mutations. medications (e.g., amiodarone, FLU-
oxetine, haloperidol, sotalol) may
PRECAUTIONS increase risk of QTc prolongation.
Contraindications: Hypersensitivity to Strong CYP3A inducers (e.g., carBA-
osimertinib. Cautions: Baseline anemia, Mazepine, phenytoin, rifAMPin) may
lymphopenia, neutropenia, thrombocyto- decrease concentration/effect. Strong
penia; COPD, heart disease (bradycardia, CYP3A inhibitors (e.g., clarithro-
cardiomyopathy, heart block, HF, recent mycin, ketoconazole, ritonavir) may
MI), pts at risk for QTc interval prolonga- increase concentration/risk of adverse
tion or ventricular arrhythmia (congenital effects. May decrease the therapeutic
long QT syndrome, history for QT pro- effect of BCG (intravesical), vaccines
longation, medications that prolong QT (live). May increase adverse/toxic effects

underlined – top prescribed drug


osimertinib 883
of belimumab, natalizumab, vac- QTc interval prolongation with symp-
cines (live). HERBAL: St. John’s wort toms of life-threatening arrhythmia:
may decrease concentration/effect. Echi- Permanently discontinue. Asymptom-
nacea may diminish therapeutic effect. atic, absolute decrease in left ven-
FOOD: None known. LAB VALUES: May tricular ejection fraction (LVEF)
decrease serum sodium, magnesium; Hgb, of 10% from baseline and below
Hct, lymphocytes, neutrophils, platelets, 50%: Withhold treatment for up to 4
RBCs. May decrease diagnostic effect of wks. Resume treatment if improved to
Coccidioides immitis skin test. baseline. If not improved to baseline,
permanently discontinue.
AVAILABILITY (Rx)
Tablets: 40 mg, 80 mg. Pulmonary Toxicity
Interstitial lung disease/pneumoni-
ADMINISTRATION/HANDLING tis: Permanently discontinue.
PO
Other Toxicities
• Tablets are hazardous; use cytotoxic Any Grade 3 or higher reaction:
precautions during handling and disposal. Withhold treatment for up to 3 wks.
Recommend single gloving when handling Resume treatment at 80 mg once daily or
intact tablets; double gloving, protective 40 mg once daily if improved to Grade 2
gown when handling liquid prepara- or lower within 3 wks. If not improved
tions. • Do not divide, crush, cut, or within 3 wks, permanently discontinue.
ultrasonicate tablets. • Give without Concomitant use of strong CYP3A4
regard to food. • If a dose is missed, skip inducers: Start dose at 160 mg once
missed dose and administer the next dose daily. May decrease dose to 80 mg once
on schedule. • Pts with dysphagia: daily if strong CYP3A4 inducer has been
Disperse tablet in 60 mL of water (noncar- O
discontinued for at least 3 wks.
bonated) only. • Stir until dissipated into
small pieces (does not completely dis- Dosage in Renal/Hepatic Impairment
solve). • Deliver orally or via gastric Mild to moderate impairment: No dose
tube. • Rinse container with 120–240 adjustment. Severe impairment: Not
mL of water and administer any remaining specified; use caution.
drug residue. After oral administration of
residue, instruct pt to thoroughly rinse SIDE EFFECTS
mouth with water and swallow. Frequent (42%–17%): Diarrhea, rash
(generalized, erythematous, macular,
INDICATIONS/ROUTES/DOSAGE maculopapular, papular, pustular),
Non–Small-Cell Lung Cancer erythema, folliculitis, acne, dermatitis,
PO: ADULTS, ELDERLY: 80 mg once daily. acneiform dermatitis, dry skin, eczema,
Continue until disease progression or skin fissures, xerosis, nail disorders
unacceptable toxicity. (inflammation, tenderness, discolor-
ation, dystrophy, infection, ridging, ony-
Dose Modification
choclasis, onycholysis, onychomadesis,
Based on Common Terminology Criteria paronychia), dry eye, blurry vision, kera-
for Adverse Events (CTCAE). titis, cataract, eye irritation, blepharitis,
Cardiac Toxicity eye pain, increased lacrimation, vitre-
QTc interval greater than 500 msec ous floaters, nausea. Occasional (16%–
on at least two separate ECGs: With- 10%): Decreased appetite, constipation,
hold treatment until QTc interval is less pruritus, cough, fatigue, back pain, sto-
than 481 msec or recovers to baseline. matitis, headache.
Once resolved, resume at 40 mg once daily.

Canadian trade name Non-Crushable Drug High Alert drug


884 oxaliplatin

ADVERSE EFFECTS/TOXIC PATIENT/FAMILY TEACHING


REACTIONS • Blood levels, echocardiograms will
Anemia, leukopenia, neutropenia, throm- be routinely monitored. • Treatment
bocytopenia are expected responses to may cause life-threatening adverse ef-
therapy. Interstitial lung disease/pneumo- fects. Report symptoms of abnormal
nitis reported in 3% of pts. May cause QTc heartbeats (dizziness, fainting, light-
interval prolongation (up to 3% of pts); headedness, palpitations), heart failure
cardiac toxicities including cardiomyopa- (shortness of breath, fast or slow heart
thy (1% of pts), decreased LVEF (2% of rate, exercise intolerance, swelling of
pts); other adverse effects including CVA, the ankles or legs), severe lung inflam-
intracranial hemorrhage; pneumonia mation (difficulty breathing, cough with
(4% of pts); venous thromboembolism fever, lung pain). • Avoid pregnancy;
including pulmonary embolism, jugular treatment may cause birth defects. Fe-
venous thrombosis, DVT (7% of pts). male pts of childbearing potential
should use effective contraception dur-
NURSING CONSIDERATIONS ing treatment and for at least 6 wks after
last dose. Male pts with female partners
BASELINE ASSESSMENT
of childbearing potential should use
Obtain CBC, BMP, serum magnesium; condoms, abstinence during treatment
vital signs; ECG. Confirm presence of and for at least 4 mos after last dose. Do
T790M mutation in tumor specimen not breastfeed during therapy and for at
prior to initiation. Obtain pregnancy test least 2 wks after last dose. • Treat-
in females of reproductive potential. Re- ment may cause blood clots in the arms,
ceive full medication history and screen legs, lungs, or brain. Immediately re-
for interactions. Question history of CVA, port symptoms of stroke (difficulty
O DVT, pulmonary embolism, pulmonary speaking, confusion, paralysis, vision
disease, cardiac disease. Obtain baseline loss), lung embolism (difficulty breath-
echocardiogram to assess LVEF. Obtain ing, fast heart rate, chest pain), blood
visual acuity. Screen for active infection. clots in the arms or legs (pain/swell-
Offer emotional support. ing). • Do not take any newly pre-
INTERVENTION/EVALUATION scribed medications unless approved by
doctor who originally started treat-
Monitor CBC for cytopenias; BMP, serum
ment. • Avoid crowds, people with ac-
magnesium for electrolyte abnormalities.
tive infection. • Do not take herbal
Pts with cough, dyspnea, fever, worsen-
supplements.
ing of respiratory status should be in-
vestigated for interstitial lung disease/
pneumonitis. Pts with sudden chest pain,
dyspnea, hypoxia, tachycardia should
be evaluated for pulmonary embolism.
oxaliplatin
Monitor for symptoms of DVT (leg or
ox-al-i-pla-tin
arm pain/swelling); CVA, intracranial
(Eloxatin )
hemorrhage (aphasia, altered LOC, facial
droop, headache, hemiplegia, seizures). j BLACK BOX ALERT j
Anaphylactic-like reaction may
Assess LVEF by echocardiogram q3mos occur within minutes of admin-
during therapy or more frequently in pts istration; may be controlled with
suspected of HF, congestive HF. Assess for EPINEPHrine, corticosteroids,
eye pain, visual changes. Monitor for skin antihistamines.
rash/toxicities, hypersensitivity reaction. Do not confuse oxaliplatin
Diligently monitor for infection. Monitor with Aloxi, CARBOplatin, or
daily stool pattern, consistency. CISplatin.

underlined – top prescribed drug


oxaliplatin 885
uCLASSIFICATION INTERACTIONS
PHARMACOTHERAPEUTIC: Plati- DRUG: Bone marrow depressants
num-containing complex. Alkylating (e.g., cladribine) may increase myelo-
agent. CLINICAL: Antineoplastic. suppression, GI effects. Live virus vac-
cines may potentiate virus replication,
increase vaccine side effects, decrease
USES pt’s antibody response to vaccine.
Treatment of stage III colon cancer HERBAL: Echinacea may decrease
after complete resection of primary effects. FOOD: None known. LAB VAL-
tumor (in combination with infusional UES: May increase serum creatinine,
5-­fluorouracil and leucovorin); treat- bilirubin, ALT, AST, INR. May prolong pro-
ment of advanced colon cancer (in com- thrombin time.
bination with infusional 5-fluorouracil
and leucovorin). OFF-LABEL: Treatment AVAILABILITY (Rx)
of ovarian cancer, pancreatic cancer, Injection Solution: 5 mg/mL (10-mL,
hepatobiliary cancer, testicular cancer, 20-mL vials).
esophageal cancer, gastric cancer, non-
Hodgkin’s lymphoma, chronic lympho- ADMINISTRATION/HANDLING
cytic leukemia. b ALERT c Wear protective gloves dur-
ing handling of oxaliplatin. If solution
PRECAUTIONS
comes in contact with skin, wash skin
Contraindications: History of allergy to immediately with soap, water. Do not use
oxaliplatin, other platinum compounds. aluminum needles or administration sets
Cautions: Previous therapy with other that may come in contact with drug; may
antineoplastic agents; radiation, renal cause degradation of platinum com-
impairment, pregnancy, immunosup- O
pounds.
pression, presence or history of periph- b ALERT c Pt should avoid ice, drink-
eral neuropathy, elderly pts. ing cold beverages, touching cold ob-
jects during infusion and for 5 days
ACTION
thereafter (can exacerbate acute neu-
Inhibits DNA replication and transcrip- ropathy).
tion by cross-linking with DNA strands.
Cell cycle–phase nonspecific. Thera- IV
peutic Effect: Causes cellular death Reconstitution • Dilute with 250–500
(apoptosis). mL D5W (never dilute with sodium chlo-
PHARMACOKINETICS ride solution or other chloride-containing
solutions) to final concentration of
Rapidly distributed. Protein binding: 0.2–0.6 mg/mL.
90%. Undergoes rapid, extensive nonen- Rate of administration • Infuse over
zymatic biotransformation. Excreted in 2–6 hrs.
urine. Half-life: 391 hrs. Storage • Do not freeze. • Protect
LIFESPAN CONSIDERATIONS from light. • Store vials at room tem-
perature. • After dilution, solution is
Pregnancy/Lactation: If possible, avoid stable for 6 hrs at room temperature, 24
use during pregnancy, esp. first trimester. hrs if refrigerated.
May cause fetal harm. Breastfeeding not
recommended. Children: Safety and effi- IV INCOMPATIBILITIES
cacy not established. Elderly: Increased
Do not infuse oxaliplatin with alkaline
incidence of diarrhea, dehydration, hypo-
medications.
kalemia, fatigue.

Canadian trade name Non-Crushable Drug High Alert drug


886 OXcarbazepine

IV COMPATIBILITIES discontinuation. Hypersensitivity reaction


Dexamethasone, diphenhydrAMINE (rash, urticaria, pruritus) occurs rarely.
(Benadryl), granisetron (Kytril), ondan-
NURSING CONSIDERATIONS
setron (Zofran), palonosetron (Aloxi).
BASELINE ASSESSMENT
INDICATIONS/ROUTES/DOSAGE
Obtain baseline renal function, WBC,
Refer to individual protocols. platelet count. Question medical history
b ALERT c Pretreat pt with antiemetics. as listed in Precautions. Offer emotional
Repeat courses should not be given more support.
frequently than every 2 wks.
INTERVENTION/EVALUATION
Colon Cancer, Advanced
Monitor for decrease in WBC, platelets
IV: ADULTS: 85 mg/m2 q2wks until dis-
(myelosuppression is minimal). Monitor
ease progression or unacceptable toxic-
daily pattern of bowel activity, stool con-
ity (in combination with fluorouracil/
sistency. Monitor for diarrhea, GI bleed-
leucovorin).
ing (bright red, black tarry stool), signs of
Colon Cancer, Stage III (adjuvant therapy) neuropathy. Pt should avoid ice or drinking,
IV: ADULTS: 85 mg/m2 q2wks for holding glass of cold liquid during IV infu-
total of 6 months (in combination with sion and for 5 days following completion of
fluorouracil/leucovorin). infusion; may precipitate/exacerbate neu-
ropathy (occurs within hrs or 1–2 days of
Dosage in Renal Impairment dosing, lasts up to 14 days). Maintain strict
CrCl less than 30 mL/min: Reduce I&O. Assess oral mucosa for stomatitis.
dose to 65 mg/m2.
PATIENT/FAMILY TEACHING
O Dosage in Hepatic Impairment • Promptly report fever, sore throat,
No dose adjustment. signs of local infection, unusual bruising/
bleeding from any site, persistent diar-
SIDE EFFECTS rhea, difficulty breathing. • Do not
Frequent (76%–20%): Peripheral/sensory have immunizations without physician’s
neuropathy (usually occurs in hands, feet, approval (drug lowers resistance).
perioral area, throat but may present as: • Avoid contact with those who have re-
jaw spasm, abnormal tongue sensation, cently taken oral polio vaccine. • Avoid
eye pain, chest pressure, difficulty walk- cold drinks, ice, cold objects (may pro-
ing, swallowing, writing), nausea, fatigue, duce neuropathy).
diarrhea, vomiting, constipation, abdomi-
nal pain, fever, anorexia. Occasional
(14%–10%): Stomatitis, earache, insom-
nia, cough, difficulty breathing, back-
ache, edema. Rare (7%–3%): Dyspepsia,
OXcarbazepine
dizziness, rhinitis, flushing, alopecia.
ox-kar-baz-e-peen
ADVERSE EFFECTS/TOXIC (Oxtellar XR, Trileptal)
REACTIONS Do not confuse OXcarbaz-
epine with carBAMazepine, or
Peripheral/sensory neuropathy can
Trileptal with TriLipix.
occur without any prior event by drink-
ing or holding a glass of cold liquid uCLASSIFICATION
during IV infusion. Pulmonary fibro-
PHARMACOTHERAPEUTIC: Car-
sis (characterized as nonproductive
boxamide derivative, anticonvulsant.
cough, dyspnea, crackles, radiologic
CLINICAL: Anticonvulsant.
pulmonary infiltrates) may warrant drug

underlined – top prescribed drug


OXcarbazepine 887

USES increase serum alkaline phosphatase,


Immediate-Release: Monotherapy, ad- ALT, AST. May decrease serum sodium.
junctive therapy in treatment of partial
AVAILABILITY (Rx)
seizures in adults. Monotherapy in chil-
dren 4 yrs and older, adjunctive therapy Oral Suspension: 300 mg/5 mL. Tab-
in children 2 yrs and older. Extended- lets: 150 mg, 300 mg, 600 mg.
Release: Treatment of partial seizures in Tablets, Extended-Release: 150 mg,
adults and children 6 yrs and older. OFF- 300 mg, 600 mg.
LABEL: Treatment of neuropathic pain,
bipolar disorder. ADMINISTRATION/HANDLING
PO
PRECAUTIONS • Give without regard to food. Do not
Contraindications: Hypersensitivity to break, crush, dissolve, or divide
OXcarbazepine. Cautions: Renal impair- extended-release tablets. Swallow whole.
ment, sensitivity to carBAMazepine, pts at
increased risk for suicide. INDICATIONS/ROUTES/DOSAGE
Adjunctive Treatment of Seizures
ACTION PO: ADULTS, ELDERLY: (Immediate-
Blocks sodium channels, stabilizing Release): Initially, 600 mg/day in 2
hyperexcited neural membranes, inhib- divided doses. May increase by up to
iting repetitive neuronal firing, dimin- 600 mg/day at wkly intervals. Maxi-
ishing synaptic impulses. Therapeutic mum: 2,400 mg/day. Usual main-
Effect: Prevents seizures. tenance dose: 600 mg twice daily.
CHILDREN 4–16 YRS: Initially, 8–10 mg/
PHARMACOKINETICS kg in 2 divided doses. Maximum: 600
Completely absorbed from GI tract. mg/day. Increase dose slowly over O
Metabolized in liver. Protein binding: 2 wks. Maintenance (based on
40%. Primarily excreted in urine. Half- weight): CHILDREN WEIGHING MORE
life: 2 hrs; metabolite, 6–10 hrs. THAN 39 KG: 1,800 mg/day in 2 divided
doses; CHILDREN WEIGHING 29.1–39
LIFESPAN CONSIDERATIONS KG: 1,200 mg/day in 2 divided doses;
Pregnancy/Lactation: Crosses pla- CHILDREN WEIGHING 20–29 KG: 900 mg/
centa. Distributed in breast milk. Chil- day in 2 divided doses. CHILDREN 2–3
dren: Safety and efficacy not established in YRS: Initially, 8–10 mg/kg/day in 2
children younger than 2 yrs. Elderly: Age- divided doses. Maximum: 600 mg/day
related renal impairment may require dos- in 2 divided doses. Increase dose slowly
age adjustment. over 2 wks up to a maximum of 60 mg/
kg/day in 2 divided doses. (Extended-
INTERACTIONS Release): ADULTS: Initially, 600 mg
DRUG: Alcohol, CNS depressants once daily. May increase by 600 mg/day
(e.g., LORazepam, morphine, zol- at wkly intervals. Range: 1,200–2,400
pidem) may have additive sedative effect. mg/day. ELDERLY: Initially, 300–450
May decrease effectiveness of oral con- mg/day. May increase by 300–450 mg/
traceptives, dolutegravir, doravirine, day at wkly intervals to desired clinical
elvitegravir, rilpivirine, simeprevir, response. Range: Up to 2,400 mg/day.
sofosbuvir, tenofovir alafenamide.
May increase serotonergic effect of Conversion to Monotherapy
selegiline. May increase concentra- PO: ADULTS, ELDERLY: (Immediate-
tion, risk of toxicity of PHENobarbital, Release): 600 mg/day in 2 divided doses
phenytoin. HERBAL: None significant. (while decreasing concomitant anticon-
FOOD: None known. LAB VALUES: May vulsant over 3–6 wks). May increase by

Canadian trade name Non-Crushable Drug High Alert drug


888 oxybutynin
600 mg/day at wkly intervals up to 2,400 pulse rate, headache, nausea, vomiting,
mg/day. CHILDREN 4–16 YRS: Initially, diarrhea. Suicidal ideation occurs rarely.
8–10 mg/kg/day in 2 divided doses with
simultaneous initial reduction of dose of NURSING CONSIDERATIONS
concomitant antiepileptic over 3–6 wks. BASELINE ASSESSMENT
May increase by maximum of 10 mg/kg/
day at wkly intervals (see below for rec- Review history of seizure disorder (type,
ommended daily dose by weight). onset, intensity, frequency, duration,
LOC), drug history (esp. other anticon-
Initiation of Monotherapy vulsants). Provide safety precautions;
PO: ADULTS, ELDERLY: (Immediate- quiet, dark environment.
Release): 600 mg/day in 2 divided INTERVENTION/EVALUATION
doses. May increase by 300 mg/day every
3 days up to 1,200 mg/day. CHILDREN Assist with ambulation if dizziness, ataxia
4–16 YRS: Initially, 8–10 mg/kg/day in 2
occur. Assess for visual abnormalities,
divided doses. Increase at 3-day intervals headache. Monitor serum sodium. Assess
by 5 mg/kg/day to achieve maintenance for signs of hyponatremia (nausea, mal-
dose by weight as follows: aise, headache, lethargy, confusion). Assess
for clinical improvement (decrease in in-
Weight Dosage
tensity, frequency of seizures). Monitor for
70+ kg 1,500–2,100 mg/day worsening depression, suicidal ideation.
60–69 kg 1,200–2,100 mg/day
50–59 kg 1,200–1,800 mg/day PATIENT/FAMILY TEACHING
41–49 kg 1,200–1,500 mg/day
35–40 kg 900–1,500 mg/day
• Do not abruptly stop taking medica-
25–34 kg 900–1,200 mg/day tion (may increase seizure activ-
20–24 kg 600–900 mg/day ity). • Report if rash, nausea, head-
O ache, dizziness occurs. • May need
periodic blood tests. • Avoid tasks that
Dosage in Renal Impairment require alertness, motor skills until re-
Mild to moderate impairment: No sponse to drug is established. • Avoid
dose adjustment. CrCl less than 30 mL/ alcohol. • May decrease effectiveness
min: Give 50% of normal starting dose, of oral contraceptives.
then titrate slowly to desired dose.
Dosage in Hepatic Impairment
Mild to moderate impairment: No dose oxybutynin
adjustment. Severe impairment: Use
caution with immediate-release; not recom- ox-i-bue-ti-nin
mended with extended-release. (Ditropan XL, Gelnique, Oxytrol for
Women)
SIDE EFFECTS Do not confuse oxybutynin with
Frequent (22%–13%): Dizziness, nausea, OxyContin.
headache. Occasional (7%–5%): Vomit-
ing, diarrhea, ataxia (muscular inco- uCLASSIFICATION
ordination), nervousness, dyspepsia, PHARMACOTHERAPEUTIC: Anticho-
constipation. Rare (4%): Tremor, rash, linergic. CLINICAL: Urinary antispas-
back pain, epistaxis, sinusitis, diplopia. modic.
ADVERSE EFFECTS/TOXIC
REACTIONS USES
Clinically significant hyponatremia may Relief of symptoms (urgency, inconti-
occur, manifested as leg cramping, hypo- nence, frequency, nocturia, urge incon-
tension, cold/clammy skin, increased tinence) associated with uninhibited
underlined – top prescribed drug
oxybutynin 889
neurogenic bladder, reflex neurogenic may increase anticholinergic effects.
bladder. Extended-Release (addi- HERBAL: None significant. FOOD: None
tional): Treatment of symptoms associ- known. LAB VALUES: None significant.
ated with detrusor overactivity due to
neurologic disorder (e.g., spina bifida). AVAILABILITY (Rx)
Syrup: 5 mg/5 mL. Tablets: 5 mg. Topi-
PRECAUTIONS cal Gel (10%): (Gelnique): 100 mg/unit
Contraindications: Hypersensitivity to oxy- dose sachet. Transdermal: (Oxytrol for
butynin. Pts with or at risk for uncontrolled Women): 3.9 mg/24 hrs.
narrow-angle glaucoma, urinary retention, Tablets, Extended-Release: 5 mg, 10
gastric retention, or conditions with severely mg, 15 mg.
decreased GI motility. Cautions: Renal/
hepatic impairment, pts with bladder out- ADMINISTRATION/HANDLING
flow obstruction, treated narrow-angle PO
glaucoma, hyperthyroidism, coronary • Give without regard to food.
artery disease, HF, hypertension, arrhyth- • Extended-release tablet must be swal-
mias, prostatic hyperplasia, myasthenia lowed whole; do not break, crush, dis-
gravis, reduced GI motility, GI obstructive solve, or divide.
disorder, gastroesophageal reflux.
Transdermal
ACTION • Apply patch to dry, intact skin on abdo-
Direct antispasmodic effect on smooth men, hip, buttock. • Use new application
muscle; inhibits action of acetylcho- site for each new patch; avoid reapplica-
line on smooth muscle. Therapeutic tion to same site within 7 days. • Normal
Effect: Increases bladder capacity, exposure to water (e.g., bathing, swim-
delays desire to void. Decreases urgency ming) should not affect patch. O
and frequency. Topical Gel
PHARMACOKINETICS • Gelnique: Apply contents of 1 sachet
once daily to dry, intact skin on abdomen,
Route Onset Peak Duration upper arms/shoulders, or thighs. • Do
PO 0.5–1 hr 3–6 hrs 6–10 hrs not bathe/shower until 1 hr after gel is
applied.
Rapidly, well absorbed from GI tract.
Metabolized in liver. Primarily excreted INDICATIONS/ROUTES/DOSAGE
in urine. Unknown if removed by hemo- Neurogenic Bladder
dialysis. Half-life: 1–2.3 hrs; metabo- PO: (Immediate-Release): ADULTS: 5
lite, 7–8 hrs. mg 2–3 times/day. May increase to
LIFESPAN CONSIDERATIONS 5 mg 4 times/day. ELDERLY: 2.5–5 mg
2–3 times/day. CHILDREN OLDER THAN 5
Pregnancy/Lactation: Unknown if YRS: 5 mg twice daily. May increase to 5
drug crosses placenta or is distributed mg 3 times/day.
in breast milk. Children: No age-related PO: (Extended-Release): ADULTS,
precautions noted in those older than 5 ELDERLY: 5–10 mg/day. May increase
yrs. Elderly: May be more sensitive to by 5-mg increments at wkly inter-
anticholinergic effects (e.g., dry mouth, vals. Maximum: 30 mg/day. CHIL-
urinary retention). DREN 6 YRS AND OLDER: Initially, 5–10
INTERACTIONS mg once daily. May increase in 5 mg
increments at wkly intervals. Maxi-
DRUG: Medications with anticholiner- mum: 20 mg/day.
gic action (e.g., aclidinium, ipratro- Transdermal: ADULTS: 3.9 mg applied
pium, tiotropium, umeclidinium) twice wkly. Apply every 3–4 days.
Canadian trade name Non-Crushable Drug High Alert drug
890 oxyCODONE
Topical gel: ADULTS, ELDERLY: (10%) j BLACK BOX ALERT jOxyContin
100 mg once daily. (controlled-release): Not intended
as an “as needed” analgesic or
Dosage in Renal/Hepatic Impairment for immediate postop pain control.
No dose adjustment. Extended-release should not
be crushed, broken, or chewed
(otherwise leads to rapid release
SIDE EFFECTS and absorption of potentially
Frequent: Constipation, dry mouth, fatal dose). Be alert to signs of
drowsiness, decreased perspiration. Occa- abuse, misuse, and diversion. May
sional: Decreased lacrimation/salivation,
cause potentially life-threatening
respiratory depression. Prolonged
impotence, urinary hesitancy/retention, use during pregnancy can cause
suppressed lactation, blurred vision, neonatal withdrawal syndrome. Use
mydriasis, nausea/vomiting, insomnia. of CYP3A4 inhibitors may increase
effects/ cause fatal respiratory
ADVERSE EFFECTS/TOXIC depression.
REACTIONS Do not confuse oxyCODONE
Overdose produces CNS excitation (ner- with HYDROcodone, oxybutynin,
vousness, restlessness, hallucinations, or oxyMORphone, OxyCONTIN
irritability), hypotension/hypertension, with MS Contin or oxybutynin,
confusion, tachycardia, facial flushing, or Roxicodone with Roxanol.
respiratory depression. FIXED-COMBINATION(S)
NURSING CONSIDERATIONS Combunox: oxyCODONE/ibupro-
fen (an NSAID): 5 mg/400 mg. En-
BASELINE ASSESSMENT docet: oxyCODONE/acetaminophen
Assess degree of dysuria, urgency, fre- (a nonnarcotic analgesic): 5 mg/325
O quency, incontinence. Question medical mg, 7.5 mg/325 mg, 7.5 mg/500
history as listed in Precautions. mg, 10 mg/325 mg, 10 mg/650 mg.
Magnacet: oxyCODONE/acetamin-
INTERVENTION/EVALUATION
ophen (a nonnarcotic analgesic):
Monitor for symptomatic relief. Monitor 2.5 mg/400 mg, 7.5 mg/400 mg,
I&O; palpate bladder for urine retention. 10 mg/400 mg. Percocet: oxyCO-
Monitor daily pattern of bowel activity, DONE/acetaminophen: 2.5 mg/325
stool consistency. mg, 5 mg/325 mg, 5 mg/500 mg,
PATIENT/FAMILY TEACHING 7.5 mg/325 mg, 7.5 mg/500 mg, 10
mg/325 mg, 10 mg/650 mg. Perco-
• Avoid alcohol. • May cause dry
cet, Roxicet, Tylox: oxyCODONE/
mouth (sugarless candy/gum may reduce
acetaminophen (a nonnarcotic an-
effect). • Avoid tasks that require alert-
algesic): 5 mg/500 mg. Percodan:
ness, motor skills until response to drug
oxyCODONE/aspirin (a nonnarcotic
is established (may cause drowsi-
analgesic): 2.25 mg/325 mg, 4.5
ness). • Avoid strenuous activity in
mg/325 mg. Targiniq ER: oxyCO-
warm environment.
DONE/naloxone (opioid antago-
nist): 10 mg/5 mg, 20 mg/10 mg,
40 mg/20 mg. Troxyca ER: oxy-
oxyCODONE CODONE/naltrexone (an opioid an-
tagonist): 10 mg/1.2 mg, 20 mg/2.4
ox-ee-koe-done mg, 30 mg/3.6 mg, 40 mg/4.8 mg,
(Oxaydo, Oxy CONTIN, OxyIR , 60 mg/7.2 mg, 9.6 mg/80 mg. Xar-
Roxicodone, Supeudol , Xtampza temis XR: oxyCODONE/acetamino-
ER) phen (nonnarcotic analgesic): 7.5
mg/325 mg.
underlined – top prescribed drug
oxyCODONE 891
uCLASSIFICATION LIFESPAN CONSIDERATIONS
PHARMACOTHERAPEUTIC: Opioid Pregnancy/Lactation: Readily crosses
agonist (Schedule II). CLINICAL: An- placenta. Distributed in breast milk.
algesic. Respiratory depression may occur in
neonate if mother received opiates dur-
ing labor. Regular use of opiates dur-
USES ing pregnancy may produce withdrawal
Immediate-Release: Relief of acute symptoms in neonate (irritability, exces-
or chronic, moderate to severe pain sive crying, tremors, hyperactive reflexes,
(usually in combination with nonopi- fever, vomiting, diarrhea, yawning, sneez-
oid analgesics). Extended-Release: ing, seizures). Children: Paradoxical
Around-the-clock management of mod- excitement may occur. Pts younger than
erate to severe pain when continuous 2 yrs are more susceptible to respiratory
analgesic is needed. depressant effects. Elderly: Age-related
renal impairment may increase risk of
PRECAUTIONS urinary retention. May be more suscep-
Contraindications: Hypersensitivity to tible to respiratory depressant effects.
oxyCODONE. Acute or severe bronchial
asthma, hypercarbia, paralytic ileus (known INTERACTIONS
or suspected), GI obstruction, significant DRUG: Alcohol, other CNS depres-
respiratory depression. Extreme Cau- sants (e.g., LORazepam, gabapentin,
tion: CNS depression, anoxia, hypercapnia, zolpidem) may increase CNS effects,
respiratory depression, seizures, acute alco- respiratory depression, hypotension.
holism, shock, untreated myxedema, respi- Strong CYP3A4 inhibitors (clar-
ratory dysfunction. Cautions: Elevated ICP, ithromycin, ketoconazole, ritona-
hepatic/renal impairment, coma, debilitated vir) may increase concentration, toxicity. O
pts, head injury, biliary tract disease, toxic Strong CYP3A4 inducers (carBAM-
psychosis, acute abdominal conditions, azepine, phenytoin, rifAMPin) may
hypothyroidism, prostatic hypertrophy, decrease concentration/effects. MAOIs
Addison’s disease, urethral stricture, COPD, may produce serotonin syndrome,
history of substance abuse, elderly pts. a severe, sometimes fatal reaction.
HERBAL: Herbals with sedative prop-
ACTION erties (e.g., chamomile, kava kava,
Binds with opioid receptors within CNS, valerian) may increase CNS depression.
causing inhibition of ascending pain path- St. John’s wort may decrease concentra-
way. Therapeutic Effect: Alters percep- tion/effect. FOOD: Grapefruit products
tion of and emotional response to pain. may increase potential for respiratory
depression. LAB VALUES: May increase
PHARMACOKINETICS serum amylase, lipase.
Route Onset Peak Duration
PO (immedi- 10–15 0.5–1 3–6 AVAILABILITY (Rx)
ate-release) min hr hrs b ALERT c New formulation of con-
PO (controlled- 10–15 0.5–1 Up to trolled-release is intended to prevent
release) min hr 12 hrs medication from being cut, broken,
Moderately absorbed from GI tract. chewed, crushed, or dissolved to reduce
Protein binding: 38%–45%. Widely dis- risk of overdose due to tampering, snort-
tributed. Metabolized in liver. Excreted ing, or injection.
in urine. Unknown if removed by hemo- Capsules: 5 mg. Oral Concentrate: 20 mg/
dialysis. Half-life: 2–3 hrs (5 hrs mL. Oral Solution: 5 mg/5 mL. Tablets: 5
controlled-release). mg, 10 mg, 15 mg, 20 mg, 30 mg. Tablets,

Canadian trade name Non-Crushable Drug High Alert drug


892 oxyCODONE
Abuse Deterrent: (Oxaydo): 5 mg, 7.5 mg. pain. Frequent: Drowsiness, dizziness, hy-
Capsules, Extended-Release: (Xtam­ potension (including orthostatic hypoten-
pza):9 mg, 13.5 mg, 18 mg, 27 mg, 36 sion), anorexia. Occasional: Confusion,
mg. Tablets, Controlled-Release 12-Hour diaphoresis, facial flushing, urinary reten-
Abuse Deterrent: (OxyCONTIN): 10 mg, 15 tion, constipation, dry mouth, nausea, vom-
mg, 20 mg, 30 mg, 40 mg, 60 mg, 80 mg. iting, headache. Rare: Allergic reaction,
depression, paradoxical CNS hyperactivity,
ADMINISTRATION/HANDLING nervousness in children, paradoxical excite-
PO ment, restlessness in elderly, debilitated pts.
• Give without regard to food. • Con- ADVERSE EFFECTS/TOXIC
trolled-release: Swallow whole; do not REACTIONS
break, crush, dissolve, or divide. Overdose results in respiratory depres-
INDICATIONS/ROUTES/DOSAGE sion, skeletal muscle flaccidity, cold/
clammy skin, cyanosis, extreme drowsi-
Note: All doses should be titrated to ness progressing to seizures, stupor,
desired effect. Do not abruptly discontinue coma. Hepatotoxicity may occur with
in physically dependent pts. Discontinu- overdose of acetaminophen component of
ation: (Immediate-Release): Reduce fixed-combination product. Tolerance to
dose by 25%-50% q2-4 days while analgesic effect, physical dependence may
monitoring for withdrawal; (Extended- occur with repeated use. Antidote: Nal-
Release): Gradually titrate downward.
oxone (see Appendix J for dosage).
Analgesia
PO: (Immediate-Release): ADULTS, NURSING CONSIDERATIONS
ELDERLY: Initially, 5–15 mg q4–6h as
O needed. Range: 5–20 mg/dose. CHILDREN BASELINE ASSESSMENT
(GREATER THAN 6 MOS) 50 KG OR GREATER: Assess onset, type, location, duration of
Initially, 5–10 mg q4–6h. Maximum: pain. Effect of medication is reduced if
20 mg/dose. LESS THAN 50 KG: 0.1–0.2 full pain recurs before next dose. Obtain
mg/kg/dose q4–6h. Maximum dose vital signs before giving medication. If
range: 5–10 mg. respirations are 12/min or less (20/min
or less in children), withhold medica-
Opioid Naive tion, contact physician.
PO: (Controlled-Release): ADULTS,
ELDERLY: (Tablets): Initially, 10 mg q12h. INTERVENTION/EVALUATION
(Capsules): Initially, 9 mg q12h. Palpate bladder for urinary retention.
b ALERT c To convert from other Monitor daily pattern of bowel activity,
o­ pioids or nonopioid analgesics to oxyCO- stool consistency. Initiate deep breathing,
DONE controlled-release, refer to Oxy- coughing exercises, esp. in pts with pul-
CONTIN package insert. Dosages are monary impairment. Monitor pain relief,
reduced in pts with severe hepatic disease. respiratory rate, mental status, B/P, LOC.
Dosage in Renal/Hepatic Impairment PATIENT/FAMILY TEACHING
Use caution. Titrate carefully. • May cause dry mouth, drowsi-
ness. • Avoid tasks that require alert-
SIDE EFFECTS ness, motor skills until response to drug
b ALERT c Effects are dependent on dos- is established. • Avoid alcohol. • May
age amount. Ambulatory pts, pts not in se- be habit forming. • Do not chew,
vere pain may experience dizziness, nausea, crush, dissolve, or divide controlled-­
vomiting, hypotension more frequently than release tablets. • Report severe consti-
those in supine position or having severe pation, absence of pain relief.

underlined – top prescribed drug


oxytocin 893
myofibrils; increases prostaglandin pro-
oxytocin duction. Therapeutic Effect: Stimu-
lates uterine contractions.
ox-ee-toe-sin
(Pitocin) PHARMACOKINETICS
j BLACK BOX ALERT jNot to be Route Onset Peak Duration
given for elective labor induc-
tion, but can be used when there IV Immediate N/A 1 hr
is a clear medical indication for IM 3–5 min N/A 2–3 hrs
induction.
Do not confuse Pitocin with Rapidly absorbed through nasal mucous
Pitressin. membranes. Protein binding: 30%. Dis-
tributed in extracellular fluid. Metabo-
uCLASSIFICATION lized in liver, kidney. Primarily excreted
PHARMACOTHERAPEUTIC: Uterine in urine. Half-life: 1–6 min.
smooth muscle stimulant. CLINI- LIFESPAN CONSIDERATIONS
CAL: Oxytocic agent.
Pregnancy/Lactation: Used as indi-
cated, not expected to present risk of
USES fetal abnormalities. Small amounts in
Antepartum: Induction of labor in pts breast milk. Breastfeeding not recom-
with medical indication (e.g., at or near mended. Children/Elderly: Not used in
term), to stimulate reinforcement of these pt populations.
labor, as adjunct in managing incomplete INTERACTIONS
or inevitable abortion. Postpartum:
To produce uterine contractions during DRUG: Dinoprostone, ­misoprostol
third stage of labor and to control post- may increase adverse effects. HERBAL: O
partum bleeding/hemorrhage. None significant. FOOD: None known.
LAB VALUES: None significant.
PRECAUTIONS
AVAILABILITY (Rx)
Contraindications: Hypersensitivity to
Injection: (Pitocin): 10 units/mL. Injec-
oxytocin. Adequate uterine activity that
tion Solution: 30 units/500 mL.
fails to progress, cephalopelvic dispro-
portion, fetal distress without imminent ADMINISTRATION/HANDLING
delivery, grand multiparity, hyperactive or
hypertonic uterus, obstetric emergencies IV
that favor surgical intervention, prematu- Reconstitution • Dilute 10–40 units
rity, unengaged fetal head, unfavorable (1–4 mL) in 1,000 mL of 0.9% NaCl,
fetal position/presentation, when vaginal lactated Ringer’s, or D5W to provide con-
delivery is contraindicated (e.g., active centration of 10–40 milliunits/mL
genital herpes infection, invasive cervi- solution.
cal cancer, placenta previa, cord pre- Rate of administration • Give by IV
sentation). Cautions: Induction of labor infusion (use infusion device to carefully
should be for medical, not elective, rea- control rate of flow as ordered by
sons. Generally not recommended in fetal physician).
distress, hydramnios, partial placental Storage • Store at room temperature.
previa, predisposition to uterine rupture.
IV INCOMPATIBILITIES
ACTION No known incompatibilities via Y-site
Activates receptors that trigger increase administration.
in intracellular calcium levels in uterine

Canadian trade name Non-Crushable Drug High Alert drug


894 oxytocin

IV COMPATIBILITIES Lacrimation/tearing, nasal irritation, rhi-


Heparin, insulin (regular), multivita- norrhea, unexpected uterine bleeding/
mins, potassium chloride, zidovudine. contractions.

INDICATIONS/ROUTES/DOSAGE ADVERSE EFFECTS/TOXIC


REACTIONS
Induction or Stimulation of Labor
IV: ADULTS: 0.5–1 milliunit/min. May Hypertonicity may occur with tearing
gradually increase in increments of 1–2 of uterus, increased bleeding, abruptio
milliunits/min q30–60 minutes until placentae (i.e., placental abruption),
desired contraction pattern is estab- cervical/vaginal lacerations. Fetal: Bra-
lished. Rates greater than 9–10 milli- dycardia, CNS/brain damage, trauma due
units/min are rarely required. to rapid propulsion, low Apgar score at 5
min, retinal hemorrhage occur rarely. Pro-
Abortion longed IV infusion of oxytocin with exces-
IV: ADULTS: (Midterm elective abor- sive fluid volume has caused severe water
tion): 10–20 milliunits/min. Maxi- intoxication with seizures, coma, death.
mum: 30 units/12-hr dose. (Incomplete,
inevitable, or elective abortion): 10
units as IV infusion after suction or a sharp NURSING CONSIDERATIONS
curettage. BASELINE ASSESSMENT
Control of Postpartum Bleeding Assess baselines for vital signs, B/P, fetal
IV infusion: ADULTS: 5–10 units may heart rate. Determine frequency, dura-
be given initially and can be followed by tion, strength of contractions.
a maintenance infusion of 10–40 units INTERVENTION/EVALUATION
O in 1,000 mL IV fluid at rate sufficient to
sustain uterine contractions and control Monitor B/P, pulse, respirations, fetal
uterine atony. heart rate, intrauterine pressure, con-
IM: ADULTS: 10 units (total dose) after
tractions (duration, strength, frequency)
delivery. q15min. Notify physician of contractions
that last longer than 1 min, occur more
Dosage in Renal/Hepatic Impairment frequently than every 2 min, or stop.
No dose adjustment. Maintain careful I&O; be alert to potential
water intoxication. Check for blood loss.
SIDE EFFECTS
PATIENT/FAMILY TEACHING
Occasional: Tachycardia, premature
ventricular contractions, hypoten- • Keep pt, family informed of labor
sion, nausea, vomiting. Rare: Nasal: progress.

underlined – top prescribed drug


PACLitaxel 895
Cautions:Hepatic impairment, severe
PACLitaxel neutropenia, peripheral neuropathy.

pak-li-tax-el ACTION
(Abraxane, Apo-Paclitaxel ) Increases action of tubulin dimers; sta-
j BLACK BOX ALERT j Myelo- bilizes existing microtubules; inhibits
suppression is a major dose-limiting their disassembly; interferes with late G2
toxicity. Must be administered by mitotic phase. Therapeutic Effect: In-
certified chemotherapy personnel.
Severe hypersensitivity reactions hibits cellular mitosis, replication.
reported.
Do not confuse PACLitaxel with PHARMACOKINETICS
DOCEtaxel, PARoxetine, or Paxil. Does not readily cross blood-brain bar-
rier. Protein binding: 89%–98%. Metabo-
uCLASSIFICATION lized in liver. Excreted in bile/feces (71%),
PHARMACOTHERAPEUTIC: Taxane urine (14%). Not removed by hemodialy-
derivative, antimitotic agent. CLINI- sis. Half-life: 3-hr infusion: 13.1–20.2
CAL: Antineoplastic. hrs; 24-hr infusion: 15.7–52.7 hrs.
LIFESPAN CONSIDERATIONS
USES Pregnancy/Lactation: May cause fetal
Conventional: Treatment of node-posi- harm. Unknown if distributed in breast milk.
tive breast cancer, metastatic breast can- Avoid use in pregnancy. Children: Safety
cer after failure of combination therapy or and efficacy not established. Elderly: No
relapse within 6 mos of adjuvant therapy; age-related precautions noted.
subsequent therapy for advanced ovarian
cancer or as first-line therapy (in combi- INTERACTIONS
nation with CISplatin). Treatment of AIDS- DRUG: Strong CYP3A4 inhibitors (e.g.,
related Kaposi’s sarcoma; non–small-cell clarithromycin, ketoconazole, ritona- P
lung cancer (NSCLC) as first-line therapy vir) may increase concentration/effect.
(in combination with CISplatin). Abrax- Strong CYP3A4 inducers (e.g., carBA-
ane: Treatment of breast cancer after Mazepine, phenytoin, rifAMPin) may
failure of combination chemotherapy or decrease effect. Bone marrow depres-
relapse within 6 mos of adjuvant chemo- sants (e.g., cladribine) may increase my-
therapy. First-line treatment of metastatic elosuppression. Strong CYP2C8 inhibi-
adenocarcinoma of pancreas. Treatment tors (e.g., gemfibrozil) may increase
of locally advanced or metastatic NSCLC. concentration/effect. Live virus vaccines
OFF-LABEL: Bladder, cervical, small-cell may potentiate virus replication, increase
lung, head and neck cancers. Treatment vaccine side effects, decrease pt’s antibody
of adenocarcinoma. Abraxane: Recur- response to vaccine. HERBAL: Herbals
rent/persistent ovarian, fallopian tube, with hypotensive properties (e.g.,
primary peritoneal cancers. garlic, ginger, gingko biloba) may
increase effect. Echinacea may decrease
PRECAUTIONS therapeutic effect. St. John’s wort may
Contraindications: Hypersensitivity to decrease concentration. FOOD: None
PACLitaxel. Hypersensitivity to drugs de- known. LAB VALUES: May elevate serum
veloped with Cremophor EL (polyoxyeth- alkaline phosphatase, bilirubin, ALT, AST,
ylated castor oil). Treatment of solid triglycerides.
tumors with baseline neutrophil count
less than 1,500 cells/mm3; treatment of AVAILABILITY (Rx)
­Kaposi’s sarcoma with baseline neutro- Injection, Powder for Reconstitution (Ab-
phil count less than 1,000 cells/mm3. raxane): 100-mg vial. Injection Solu-

Canadian trade name Non-Crushable Drug High Alert drug


896 PACLitaxel
6 mg/mL (5-mL, 16.7-mL, 25-mL,
tion: Amphotericin B complex (Abelcet, Am-
50-mL vials). Bisome, Amphotec), DOXOrubicin lipo-
somal (Doxil), hydrOXYzine (Vistaril),
ADMINISTRATION/HANDLING methylPREDNISolone (SOLU-Medrol),
mitoXANTRONE (Novantrone).
IV
IV COMPATIBILITIES
b ALERT c Wear gloves during han-
dling; if contact with skin occurs, wash CARBOplatin (Paraplatin), CISplatin (Plat-
hands thoroughly with soap, water. If inol AQ), cyclophosphamide (Cytoxan),
contact with mucous membranes occurs, cytarabine (Cytosar), dacarbazine (DTIC-
flush with water. Dome), dexamethasone (Decadron),
diphenhydrAMINE (Benadryl), DOXOru-
PACLitaxel
bicin (Adriamycin), etoposide (VePesid),
Reconstitution • Dilute with 250– gemcitabine (Gemzar), granisetron (Ky-
1,000 mL 0.9% NaCl, D5W to final con- tril), HYDROmorphone (Dilaudid), lipids,
centration of 0.3–1.2 mg/mL. magnesium sulfate, mannitol, methotrex-
Rate of administration • Administer
ate, morphine, ondansetron (Zofran),
at rate per protocol (range: 1–96 hrs) potassium chloride, vinBLAStine (Velban),
through in-line filter not greater than vinCRIStine (Oncovin).
0.22 microns. • Monitor vital signs INDICATIONS/ROUTES/DOSAGE
during infusion, esp. during first Note: Premedication with dexametha-
hour. • Discontinue administration if sone, diphenhydrAMINE, and cimetidine,
severe hypersensitivity reaction occurs. famotidine, or raNITIdine recommended.
Storage • Store unopened vials at
Refer to individual protocols.
room temperature. • Reconstituted so-
lution is stable at room temperature for 72 PACLitaxel (Conventional)
hrs. • Store diluted solutions in bottles Ovarian Cancer
P or plastic bags. Administer through poly- IV: ADULTS, ELDERLY: (Previously
ethylene-lined administration sets (avoid treated): 135–175 mg/m2/dose over 3
plasticized PVC equipment or devices). hrs q3wks. (Previously untreated): 175
mg/m2 over 3 hrs q3wks (in combination
Abraxane (PACLitaxel—Protein Bound) with CISplatin) or 135 mg/m2 over 24 hrs
Reconstitution • Reconstitute each q3wks (in combination with CISplatin).
vial with 20 mL 0.9% NaCl to provide con- Breast Cancer (Adjuvant)
centration of 5 mg/mL. • Slowly inject IV: ADULTS, ELDERLY: 175 mg/m2 over 3
onto inside wall of vial; gently swirl over 2 hrs for 4 cycles (give sequentially follow-
min to avoid foaming. • Inject appropri- ing anthracycline-containing regimen).
ate amount into empty PVC-type bag. Breast Cancer (Metastatic/Relapsed)
Rate of administration • Infuse over IV: ADULTS, ELDERLY: 175 mg/m2 over 3
30 min. Do not use in-line filter. hrs q3wks.
Storage • Store unopened vials at Non–Small-Cell Lung Cancer
room temperature. • Once reconsti- IV: ADULTS, ELDERLY: 135 mg/m2 over
tuted, use immediately but may refriger- 24 hrs (in combination with CISplatin).
ate for up to 8 hrs. Kaposi’s Sarcoma (AIDS-Related)
IV: ADULTS, ELDERLY: 135 mg/m2/dose
IV INCOMPATIBILITIES over 3 hrs q3wks or 100 mg/m2/dose
b ALERT c Data for Abraxane not over 3 hrs q2wks.
known; avoid mixing with other Dosage in Renal Impairment
­medication. No dose adjustment.

underlined – top prescribed drug


PACLitaxel 897
Dosage in Hepatic Impairment Dose Modification
Transaminase Severe neutropenia (ANC less than
Level Bilirubin Dose 500 cells/mm3 for 1 wk or longer);
24-HR INFUSION severe sensory neuropathy: Re-
Less than 2 1.5 mg/dL or 135 mg/m2 duce dose to 220 mg/m2 for subse-
times ULN less quent courses. Recurrence of severe
2 to less than 1.5 mg/dL or 100 mg/m2 neutropenia, severe neuropathy:
10 times less Reduce dose to 180 mg/m2 q3wks for
ULN subsequent courses. CTCAE Grade 3
Less than 10 1.6–7.5 mg/dL 50 mg/m2 sensory neuropathy: Hold until re-
times ULN or less
solved to Grade 2 or 1, then reduce dose
3-HR INFUSION for subsequent courses. Dosage of Ab-
Less than 10 1.25 mg/dL or 175 mg/m2
raxane for serum bilirubin greater
times ULN less
Less than 10 1.26–2 times 135 mg/m2 than 1.5 mg/dL: Dose unknown.
times ULN ULN NSCLC (Locally Advanced or Metastatic)
Less than 10 2.01–5 times 90 mg/m2
IV: ADULTS, ELDERLY: 100 mg/m2 on
times ULN ULN
10 times ULN Greater than Avoid use days 1, 8, 15 of each 21-day cycle (in
or greater 5 times ULN combination with CARBOplatin).
ULN: upper limit of normal Adenocarcinoma of Pancreas
Dose Modification (Metastatic) (in combination with
Courses of PACLitaxel should be withheld gemcitabine)
until neutrophil count is 1,500 cells/mm3 IV: ADULTS, ELDERLY: 125 mg/m2 on
or more and platelet count is 100,000 days 1, 8, 15 of each 28-day cycle (in
cells/mm3 or more. combination with gemcitabine).
Dosage in Renal Impairment
Abraxane (Protein Bound)
No dose adjustment. P
Breast Cancer (Metastatic)
IV infusion: ADULTS, ELDERLY: 260 mg/
m2 q3wks.

Dosage in Hepatic Impairment


Mild Severe Impairment
Impairment
(AST Less Than Moderate
10 Times Upper Impairment (AST Less (AST More
Limit of Normal (AST Less Than Than 10 Than 10 Times
[ULN], Bilirubin 10 Times ULN, Times ULN, ULN or
1.25 Times ULN Bilirubin 1.26–2 Bilirubin 2.01–5 Bilirubin > 5
or Less) Times ULN) Times ULN) Times ULN)
Breast No ­adjustment Reduce dose to Reduce dose to 130 Not recom-
cancer 200 mg/m2 mg/m2 (may increase mended
to 200 mg/m2 in sub-
sequent cycles)
NSCLC No ­adjustment Reduce dose to Reduce dose to 50 Not recom-
75 mg/m2 mg/m2 (may increase mended
to 75 mg/m2 in sub-
sequent cycles)
Pancreatic No ­adjustment Not recom- Not recommended Not recom-
mended mended

Canadian trade name Non-Crushable Drug High Alert drug


898 palbociclib

SIDE EFFECTS
Expected (90%–70%): Diarrhea, alope-
palbociclib
cia, nausea, vomiting. Frequent (48%–
pal-boe-sye-klib
46%): Myalgia, arthralgia, peripheral
(Ibrance)
neuropathy. Occasional (20%–13%): Mu-
cositis, hypotension during infusion, uCLASSIFICATION
pain/redness at injection site. Rare
PHARMACOTHERAPEUTIC: Cyclin-
(3%): Bradycardia.
dependent kinase inhibitor. CLINI-
ADVERSE EFFECTS/TOXIC CAL: Antineoplastic.
REACTIONS
Neutropenic nadir occurs at median of 11 USES
days. Anemia, leukopenia occur commonly; Used in combination with an aromatase
thrombocytopenia occurs occasionally. Se- inhibitor (e.g., letrozole) for treatment
vere hypersensitivity reaction (dyspnea, se- of postmenopausal women and adult
vere hypotension, angioedema, generalized men with estrogen receptor–positive,
urticaria) occurs rarely. human epidermal growth factor recep-
tor 2 (HER2)–negative advanced breast
NURSING CONSIDERATIONS cancer as initial endocrine-based therapy
BASELINE ASSESSMENT for metastatic disease or in combination
with fulvestrant in women with disease
Obtain CBC (note neutrophil count), progression following endocrine therapy.
BMP, LFT prior to each course. Receive
full medication history and screen for in- PRECAUTIONS
teractions. Offer emotional support. Contraindications: Hypersensitivity to
INTERVENTION/EVALUATION palbociclib. Cautions: Baseline anemia,
lymphopenia, neutropenia, thrombocy-
P Monitor CBC, LFT, vital signs. Moni- topenia. History of pulmonary embolism.
tor for hematologic toxicity (fever, sore Avoid concomitant use of strong or mod-
throat, signs of local infections, unusual erate CYP3A inhibitors, strong or moder-
bleeding/bruising), symptoms of anemia ate CYP3A inducers.
(excessive fatigue, weakness). Monitor
daily pattern of bowel activity, stool con- ACTION
sistency; report diarrhea. Avoid IM injec- Reduces proliferation of breast cancer
tions, rectal temperatures, other traumas cell lines by preventing cellular pro-
that may induce bleeding. Hold pressure gression from G1 into S phase of cell
to injection sites for full 5 min. cycle. Combination with an aromatase
PATIENT/FAMILY TEACHING inhibitor provides increased inhibition.
Therapeutic Effect: Inhibits tumor cell
• Hair loss is reversible, but new hair growth and metastasis.
may have different color, texture. • Do
not have immunizations without physi- PHARMACOKINETICS
cian’s approval (drug lowers resis- Readily absorbed. Widely distributed.
tance). • Avoid crowds, persons with Metabolized in liver. Protein binding:
known infections. • Report signs of in- 85%. Peak plasma concentration: 6–12
fection at once (fever, flu-like symp- hrs. Steady state reached in 8 days. Ex-
toms). • Report persistent nausea/ creted in feces (74%), urine (18%).
vomiting. • Be alert for signs of periph- Half-life: 29 hrs.
eral neuropathy. • Avoid preg-
nancy. • Avoid tasks that may require LIFESPAN CONSIDERATIONS
alertness, motor skills until response to Pregnancy/Lactation: Treatment is
drug is established. indicated for postmenopausal women.
underlined – top prescribed drug
palbociclib 899
However, treatment may cause fetal harm 28-day cycle. Continue until disease pro-
when administered during pregnancy. gression or unacceptable toxicity.
Females of reproductive potential should
Breast Cancer (Disease Progression)
use effective contraception during treat-
PO: ADULTS, ELDERLY: 125 mg once daily
ment and up to 2 wks after discontinu-
ation. Unknown if distributed in breast for 21 days, then 7 days off. Repeat q28
milk. Must either discontinue drug or dis- days (in combination with fulvestrant
continue breastfeeding. Children: Safety [and an LHRH agonist if pre- or peri-
and efficacy not established. Not indicated menopausal]). Continue until disease
for this pt population. Elderly: No age- progression or unacceptable toxicity.
related precautions noted. Dose Reduction for Adverse Events
Dose Level Dose
INTERACTIONS
Recommended starting dose 125 mg/day
DRUG: Strong CYP3A inhibitors (e.g., First dose reduction 100 mg/day
clarithromycin, ketoconazole, ritona- Second dose reduction 75 mg/day
vir), moderate CYP3A inhibitors (e.g., Unable to tolerate 75 mg/ Permanently
atazanavir, ciprofloxacin) may increase day discontinue
concentration/effect; avoid use. Strong Dose Modification
CYP3A inducers (e.g., carBAMazepine, Based on Common Terminology Criteria
rifAMPin), moderate CYP3A induc- for Adverse Events (CTCAE).
ers (e.g., nafcillin) may decrease con-
centration/effect; avoid use. May decrease Hematologic Toxicities
the therapeutic effect of vaccines (live). Grade 1 or 2: No dose adjustment. Grade
May increase adverse/toxic effects of na- 3 (except lymphopenia unless associ-
talizumab, vaccines (live). HERBAL: St. ated with clinical events [e.g., oppor-
John’s wort may decrease concentration/­ tunistic infection]): No dose adjustment.
effect. Echinacea may decrease therapeu- Withhold treatment until recovery to less than
tic effect. FOOD: Grapefruit products Grade 2. Grade 3, ANC 500–1000 cells/ P
may increase concentration/effect. LAB mm3 plus fever that is greater than
VALUES: May decrease Hgb, lymphocytes, or equal to 38.5°C and/or active infec-
neutrophils, platelets, WBC. tion: Interrupt treatment (and initiation of
the next cycle) until recovery to Grade 2 or
AVAILABILITY (Rx) less. Resume at reduced dose upon starting.
Capsules: 75 mg, 100 mg, 125 mg. Nonhematologic Toxicities
ADMINISTRATION/HANDLING Grade 1 or 2: No dose adjustment.
Grade 3 or greater (if persistent de-
PO
spite optimal medical management):
• Give with food. • Administer whole; Interrupt treatment until resolved to Grade
do not break, crush, cut, or open cap- 1 or less; Grade 2 or less if the event is
sule. • If vomiting occurs after dosing, not considered a serious medical risk. Re-
do not readminister dose; give dose at sume at reduced dose upon starting.
next scheduled time.
Concomitant Use of Strong CYP3A
INDICATIONS/ROUTES/DOSAGE Inhibitors
Breast Cancer (initial endocrine-based PO: ADULTS, ELDERLY: 75 mg once daily
therapy) if unable to use alternative drug with
PO: ADULTS, ELDERLY: 125 mg once minimal CYP3A inhibition. If CYP3A in-
daily for 21 days, followed by a 7-day rest hibitor is discontinued, increase palboci-
period to complete a 28-day cycle. Use in clib dose (after 3–5 half-lives of CYP3A
combination with an aromatase inhibitor inhibitor have elapsed) to the dose used
(e.g., letrozole) once daily throughout prior to initiating strong CYP3A inhibitor.

Canadian trade name Non-Crushable Drug High Alert drug


900 paliperidone
Dosage in Renal Impairment delay in starting treatment for next cycle.
Mild to moderate impairment: No Monitor for neurotoxicity (peripheral
dose adjustment. Severe impairment: neuropathy), epistaxis. If chest pain, dys-
Not studied; use caution. pnea, tachycardia occurs, provide supple-
mental O2 and obtain radiologic testing to
Dosage in Hepatic Impairment rule out pulmonary embolism.
Mild impairment: No dose adjust­ment.
Moderate to severe impairment: Not PATIENT/FAMILY TEACHING
studied; use caution. • Blood levels will be monitored regu-
larly. • Treatment may cause fetal harm.
SIDE EFFECTS Women of childbearing potential should
Frequent (41%–21%): Fatigue, nausea, use effective contraception during treatment
alopecia, diarrhea. Occasional (16%– and up to 2 wks following discontinuation.
13%): Decreased appetite, vomiting, Immediately report suspected pregnancy.
asthenia. Do not breastfeed. • Immediately report
chest pain, difficult breathing, fast heart
ADVERSE EFFECTS/TOXIC rate, rapid breathing; may indicate life-
REACTIONS threatening blood clot in the lungs. • Re-
Anemia, leukopenia, neutropenia, throm- port symptoms of bone marrow suppres-
bocytopenia are expected responses to sion or infection such as bruising easily,
therapy. CTCAE Grade 3 neutropenia re- chills, cough, dizziness, fainting, fever,
ported in 57% of pts. The median onset shortness of breath, weakness. • Swallow
of neutropenia was 15 days. Pulmonary capsules whole; do not chew, crush, cut, or
embolism (5% of pts); upper respira- open capsules. • Take each dose with
tory tract infections including influenza, food. • Treatment may increase risk of
laryngitis, nasopharyngitis, pharyngitis, infection, nosebleeds. • Drink plenty of
rhinitis, sinusitis (31% of pts); periph- fluids. • Do not ingest grapefruit products
P eral neuropathy (31% of pts); cheilitis, or herbal supplements. • Avoid crowds,
glossitis, glossodynia, mouth ulceration, those with active infection.
stomatitis (25% of pts); epistaxis (11%
of pts) were reported.
NURSING CONSIDERATIONS
paliperidone
BASELINE ASSESSMENT pal-ee-per-i-done
Obtain baseline ANC, CBC. Confirm es- (Invega, Invega Sustenna, Invega
trogen receptor–positive, HER2-negative Trinza)
status. Verify pregnancy status before j BLACK BOX ALERT jElderly pts
with dementia-related psychosis
start of each cycle. Screen for history of are at increased risk for mortality
pulmonary embolism. Receive full medi- due to cerebrovascular events.
cation history and screen for interac-
tions. Assess hydration status. Screen for uCLASSIFICATION
active infection. Offer emotional support. PHARMACOTHERAPEUTIC: Ben-
INTERVENTION/EVALUATION zisoxazole derivative. CLINICAL:
Second-generation (atypical) anti­
Monitor ANC, CBC at start of each cycle psychotic.
and on day 14 on the first two cycles. If
any Grade 3 or 4 hematologic toxicity oc-
curs, repeat CBC 7 days after interruption
of therapy and at start of next cycle. If neu- USES
tropenia occurs specifically, recommend PO: Treatment of schizophrenia.
treatment interruption, dose reduction, or PO, IM: Treatment of schizoaffective

underlined – top prescribed drug


paliperidone 901
disorder. OFF-LABEL: Treatment of irri- concentration/effect. Herbals with sed-
tability associated with autistic disorder. ative properties (e.g., chamomile,
kava kava, valerian) may increase CNS
PRECAUTIONS depression. FOOD: None known. LAB
Contraindications: Sensitivity to paliperi- VALUES: May increase serum creatine
done, risperiDONE. Cautions: History of phosphatase, uric acid, triglycerides, ALT,
cardiac arrhythmias, mild renal impairment AST, prolactin. May decrease serum po-
(not recommended in moderate to severe tassium, sodium, protein, glucose.
impairment), diabetes, HF, active seizures
or predisposition to seizures, history of AVAILABILITY (Rx)
seizures, cardiovascular disease, congenital Injection Suspension: (Invega Sustenna):
long QT syndrome, concomitant use with 39 mg/0.25 mL, 78 mg/0.5 mL, 117
other medications that prolong QT interval, mg/0.75 mL, 156 mg/mL, 234 mg/1.5 mL.
pts at risk for aspiration pneumonia. May (Invega Trinza): 273 mg, 410 mg, 546 mg,
increase risk of stroke in pts with dementia- 819 mg.
related psychosis. CNS depression, concom- Tablets, Extended-Release: 1.5 mg,
itant use of antihypertensives, hypovolemia 3 mg, 6 mg, 9 mg.
or dehydration, high risk for suicide. Pts
with breast cancer, other prolactin-depen- ADMINISTRATION/HANDLING
dent tumors; children, adolescents. PO
• May give without regard to
ACTION food. • Do not break, crush, dissolve,
Exact mechanism unknown. May be a result or divide extended-release tablets.
of mixed central DOPamine and serotonin
antagonism. Therapeutic Effect: Sup- IM
presses behavioral response in psychosis. • Administer both initial injections (first
injection on day 1 and the second injec-
PHARMACOKINETICS tion 1 wk later) into deltoid muscle P
Absorbed from GI tract. Metabolized in (helps attain therapeutic concentration
liver. Primarily excreted in urine. Half- rapidly). • Maintenance doses may be
life: 23 hrs. given in gluteal or deltoid muscle.
LIFESPAN CONSIDERATIONS INDICATIONS/ROUTES/DOSAGE
Pregnancy/Lactation: Unknown if drug Schizophrenia
crosses placenta or is distributed in breast PO: ADULTS, ELDERLY: Initially, 6 mg
milk. Children: Safety and efficacy not once daily in the morning. May in-
established. Elderly: Potential for ortho- crease dose in increments of 3 mg/
static hypotension. Age-related renal im- day at intervals of more than 5 days.
pairment may require dosage adjustment. Range: 3–12 mg/day. ADOLESCENTS
51 KG OR MORE: Initially, 3 mg once
INTERACTIONS daily. Range: 3–12 mg/day. 50 KG OR
DRUG: May decrease effects of DOPa- LESS: Initially, 3 mg once daily. Range:
mine agonists, levodopa. Alcohol, 3–6 mg/day.
CNS depressants (e.g., LORazepam, IM: (Invega Sustenna): ADULTS, EL-
morphine, zolpidem) may increase DERLY: Initially, 234 mg on day 1 fol-
CNS depression. Strong CYP3A4 in- lowed by 156 mg 1 wk later (second
ducers (e.g., carBAMazepine, phe- dose may be given 4 days before or
nytoin, rifAMPin) may decrease con- after the wkly time point). Mainte-
centration/effect. Itraconazole may nance: Following the 1-wk initiation
increase QT interval–prolonging effect. regimen, begin 117 mg monthly. Range:
HERBAL: St. John’s wort may decrease 39–234 mg (based on response and tol-

Canadian trade name Non-Crushable Drug High Alert drug


902 palonosetron
erability). Monthly maintenance dose failure, tardive dyskinesia (protrusion of
may be given 7 days before or after the tongue, puffing of cheeks, chewing/puck-
monthly time point. (Invega Trinza): ering of mouth) may occur rarely. May
273 mg to 819 mg q3mos (based on prolong QT interval.
last dose of Invega Sustenna). Three-
month IM used only after monthly IM NURSING CONSIDERATIONS
dose established for at least 4 mos. The BASELINE ASSESSMENT
last 2 mos of monthly IM should be the
same dosage strength before starting Obtain baseline renal function tests. As-
3-mo injections. sess behavior, appearance, emotional
status, response to environment, speech
Schizoaffective Disorder pattern, thought content. Screen for co-
PO: ADULTS, ELDERLY: 6 mg once daily morbidities as listed in Precautions.
in the morning. May increase in incre- INTERVENTION/EVALUATION
ments of 3 mg/day at intervals of more
than 4 days. Range: 3–12 mg/day. Monitor B/P, heart rate, weight, renal
IM: ADULTS, ELDERLY: Initially, 234 mg,
function tests, ECG. Monitor for fine
then 156 mg 1 wk later. Maintenance tongue movement (may be first sign of
range: 39–234 mg monthly (based on tardive dyskinesia). Supervise suicidal-
response and tolerability). May be given 7 risk pt closely during early therapy (as
days before or after the monthly time point. depression lessens, energy level im-
proves, increasing suicide potential).
Dosage in Renal Impairment Assess for therapeutic response (greater
Creatinine
interest in surroundings, improved self-
Clearance Oral Dosage IM Dosage
care, increased ability to concentrate, re-
laxed facial expression). Monitor for po-
50–79 mL/ Initially, 3 Initially, 156
min mg/d Maxi- mg, then
tential neuroleptic malignant syndrome
mum: 6 mg/d 117 mg 1 (fever, muscle rigidity, unstable B/P or
P pulse, altered mental status).
wk later,
then 78 mg
PATIENT/FAMILY TEACHING
monthly
10–49 mL/ Initially, 1.5 Not recom- • Avoid tasks that may require alertness,
min mg/d Maxi- mended motor skills until response to drug is es-
mum: 3 mg/d tablished. • Use caution when changing
Less than Not recom- Not recom- position from lying or sitting to stand-
10 mL/min mended mended ing. • Report trembling in fingers, al-
tered gait, unusual muscle/skeletal move-
Dosage in Hepatic Impairment ments, palpitations, severe dizziness,
No dose adjustment. fainting, swelling/pain in breasts, visual
changes, rash, difficulty in breathing.
SIDE EFFECTS
Occasional (14%–4%): Tachycardia, head­
ache, drowsiness, akathisia, anxiety, diz-
ziness, dyspepsia, nausea. palonosetron
ADVERSE EFFECTS/TOXIC pal-oh-noe-se-tron
REACTIONS (Aloxi)
Neuroleptic malignant syndrome (NMS), Do not confuse Aloxi with
hyperpyrexia, muscle rigidity, change Eloxatin or oxaliplatin, or
in mental status, unstable pulse or B/P, palonosetron with dolasetron,
tachycardia, diaphoresis, cardiac ar- granisetron, or ondansetron.
rhythmias, rhabdomyolysis, acute renal
underlined – top prescribed drug
palonosetron 903

FIXED-COMBINATION(S) RIs (e.g., citalopram, FLUoxetine,


Akynzeo: palonosetron/netupitant (a sertraline), tricyclic antidepres-
substance P/neurokinin receptor an- sants (e.g., amitriptyline, doxepin)
tagonist): 0.5 mg/300 mg. may increase risk of serotonin syndrome.
HERBAL: None significant. FOOD: None
uCLASSIFICATION known. LAB VALUES: May transiently in-
PHARMACOTHERAPEUTIC: Selective crease serum bilirubin, ALT, AST.
5-HT3 receptor antagonist. CLINI-
CAL: Antiemetic. AVAILABILITY (Rx)
Injection Solution: 0.25 mg/5 mL.
USES ADMINISTRATION/HANDLING
Prevention of acute and delayed nausea/ IV
vomiting associated with initial/repeated
courses of moderately or highly emeto- Reconstitution • Give undiluted as IV
genic chemotherapy. Prevention of push.
post­op nausea/vomiting for up to 24 hrs Rate of administration • Give IV
following surgery. push over 30 sec. Children: Infuse over
15 min. • Flush infusion line with 0.9%
PRECAUTIONS NaCl before and following administration.
Contraindications: Hypersensitivity to Storage • Store at room temperature.
palonosetron. Cautions: History of car- Solution should appear colorless, clear.
diovascular disease; congenital long QT Discard if cloudy precipitate forms.
syndrome, risk factors for QT prolonga-
tion (hypokalemia, hypomagnesemia), IV COMPATIBILITIES
medications that prolong QT interval or Famotidine (Pepcid), LORazepam (Ati-
reduce potassium/magnesium levels, pts van), midazolam (Versed), potassium
at risk for ventricular arrhythmias. chloride. P
ACTION INDICATIONS/ROUTES/DOSAGE
Antagonizes 5-HT3 receptors, blocking se- Chemotherapy-Induced Nausea/Vomiting
rotonin on both peripheral and vagal nerve IV: ADULTS, ELDERLY: 0.25 mg as single
terminals in chemoreceptor trigger zone. dose 30 min before starting chemother-
Therapeutic Effect: Decreases episodes apy. CHILDREN 1 MO TO YOUNGER THAN 17
of nausea/vomiting associated with che- YRS: 20 mcg/kg as single dose 30 min
motherapy or postoperative recovery. before starting chemotherapy. Maxi-
mum: 1.5 mg.
PHARMACOKINETICS
Protein binding: 52%. Metabolized in liver. Postop Nausea/Vomiting
Excreted in urine. Half-life: 40 hrs. IV: ADULTS, ELDERLY: 0.075 mg over 10
sec immediately before induction of an-
LIFESPAN CONSIDERATIONS esthesia.
Pregnancy/Lactation: Unknown if dis-
Dosage in Renal/Hepatic Impairment
tributed in breast milk. Children: Safety
and efficacy not established. Elderly: No No dose adjustment.
age-related precautions noted. SIDE EFFECTS
INTERACTIONS Occasional (9%–5%): Headache, consti-
DRUG: FentaNYL, lithium, MAOIs pation. Rare (less than 1%): Diarrhea,
(e.g., phenelzine, selegiline), SNRIs dizziness, fatigue, abdominal pain, in-
(e.g., DULoxetine, venlafaxine), SS- somnia.

Canadian trade name Non-Crushable Drug High Alert drug


904 pamidronate

ADVERSE EFFECTS/TOXIC
REACTIONS pamidronate
Overdose may produce combination
pam-id-roe-nate
of CNS stimulation, depressant effects.
(Aredia )
May prolong QT interval. 5-HT3 recep-
Do not confuse Aredia with
tor antagonists are known to potentiate
Adriamycin, or pamidronate
serotonin syndrome, esp. in pts taking
with alendronate, ibandronate,
serotonergic medications.
or risedronate.
NURSING CONSIDERATIONS uCLASSIFICATION
BASELINE ASSESSMENT PHARMACOTHERAPEUTIC: Bispho-
Obtain BMP, serum magnesium in pts sphonate. CLINICAL: Hypocalcemic.
at risk for hypokalemia, hypomagnese-
mia, QT interval prolongation. Assess
for signs of dehydration due to excessive USES
vomiting (poor skin turgor, dry mucous Treatment of moderate to severe hypercal-
membranes). Question history of cardiac cemia associated with malignancy (with/
disease, long QT syndrome, cardiac ar- without bone metastases). Treatment of
rhythmias. Screen for concomitant home moderate to severe Paget’s disease. Treat-
medications that prolong QT interval, in- ment of osteolytic bone lesions of multiple
crease risk of serotonin syndrome. Pro- myeloma or bone metastases of breast can-
vide emotional support. cer. OFF-LABEL: Inhibits bone resorption in
osteogenesis imperfecta, treatment of bone
INTERVENTION/EVALUATION metastases of thyroid cancer, prevention of
Monitor for occurrence of nausea/vom- bone loss associated with androgen depri-
iting. Assess for dehydration if excessive vation treatment in prostate cancer.
P vomiting occurs (poor skin turgor, dry
mucous membranes, longitudinal fur- PRECAUTIONS
rows in tongue). Monitor BMP, serum Contraindications: Hypersensitivity to
magnesium; ECG in pts suspected of ar- pamidronate, other bisphosphonates
rhythmia, QT interval prolongation. As- (e.g., risedronate, alendronate). Cau-
sess for symptoms of serotonin syndrome tions: Renal impairment, concurrent use
(e.g., altered mental status, tachycardia, with other nephrotoxic medications, his-
labile B/P, diaphoresis, hyperthermia, tory of thyroid surgery. Preexisting ane-
tremor, hyperreflexia, diarrhea, sei- mia, leukopenia, thrombocytopenia.
zures). Monitor for hypersensitivity
­reaction. ACTION
PATIENT/FAMILY TEACHING
Inhibits bone resorption, decreases min-
eralization by disrupting activity of os-
• Relief from nausea/vomiting generally teoclasts. Therapeutic Effect: Lowers
occurs shortly after drug administra- serum calcium concentration.
tion. • Report symptoms of serotonin
overproduction such as confusion, ex- PHARMACOKINETICS
cessive talking, fever, hallucinations, Route Onset Peak Duration
headache, hyperactivity, insomnia, racing
IV 24–48 hrs 3–7 days N/A
thoughts, seizure activity, sexual dysfunc-
tion, tremors. • Report persistent vom- After IV administration, rapidly absorbed
iting. • Report palpitations, light-head- by bone. Slowly excreted unchanged in
edness, fainting; allergic reactions of any urine. Unknown if removed by hemodi-
kind. alysis. Half-life: 21–35 hrs.

underlined – top prescribed drug


pamidronate 905

LIFESPAN CONSIDERATIONS is stable for 24 hrs if refrigerated; IV so-


Pregnancy/Lactation: Unknown if lution is stable for 24 hrs after dilution.
crosses placenta. Recommend discontin-
IV INCOMPATIBILITIES
uation of drug as early as possible before
a planned pregnancy. Unknown if fetal Calcium-containing IV fluids.
harm can occur. Unknown if distributed
in breast milk. Children: Safety and INDICATIONS/ROUTES/DOSAGE
efficacy not established. Elderly: May Hypercalcemia of Malignancy
become overhydrated. Careful monitor- IV infusion: ADULTS, ELDERLY: Moder-
ing of fluid and electrolytes indicated; ate hypercalcemia (corrected serum
recommend dilution in smaller volume. calcium level 12–13.5 mg/dL): 60–
90 mg as a single dose over 2–24 hrs.
INTERACTIONS ­Severe hypercalcemia (corrected
DRUG: NSAIDs (e.g., ibuprofen, ke- serum calcium level greater than
torolac, naproxen) may increase ad- 13.5 mg/dL): 90 mg as a single dose
verse/toxic effects (e.g., increased risk over 2–24 hrs.
of ulcer). Proton pump inhibitors
Paget’s Disease
(e.g., omeprazole, pantoprazole)
IV infusion: ADULTS, ELDERLY: 30 mg/
may decrease effect. Aminoglycosides
day over 4 hrs for 3 consecutive days.
(e.g., gentamicin) may increase risk of
May retreat if clinically indicated.
hypokalemia. HERBAL: None significant.
FOOD: None known. LAB VALUES: None Osteolytic Bone Lesion (Multiple
significant. Myeloma)
IV infusion: ADULTS, ELDERLY: 90 mg
AVAILABILITY (Rx) over 4 hrs once monthly.
Injection, Powder for Reconstitution: 30
mg, 90 mg. Injection Solution: 3 mg/mL, Osteolytic Bone Metastases (Breast P
6 mg/mL, 9 mg/mL. Cancer)
IV infusion: ADULTS, ELDERLY: 90 mg
ADMINISTRATION/HANDLING over 2 hrs q3–4wks.
IV Dosage in Renal Impairment
Reconstitution • Reconstitute each Not recommended.
vial with 10 mL Sterile Water for Injection
to provide concentration of 3 mg/mL or 9 Dosage in Hepatic Impairment
mg/mL. • Allow drug to dissolve before No dose adjustment.
withdrawing. • Further dilute with 250–
SIDE EFFECTS
1,000 mL sterile 0.45% or 0.9% NaCl or
D5W (1,000 mL for hypercalcemia of ma- Frequent (27%–18%): Temperature eleva-
lignancy, 500 mL for Paget’s disease, mul- tion (at least 1°C) 24–48 hrs after ad-
tiple myeloma, 250 mL for breast cancer). ministration; erythema, swelling, indura-
Rate of administration • Adequate tion, pain at catheter site in pts receiving
hydration is essential in conjunction with 90 mg; anorexia, nausea, fatigue. Occa-
pamidronate therapy (avoid overhydra- sional (10%–1%): Constipation, rhinitis.
tion in pts with potential for HF). • Ad-
ADVERSE EFFECTS/TOXIC
minister as IV infusion over 2–24 hrs for
REACTIONS
treatment of hypercalcemia; over 2 hrs
for breast cancer; over 4 hrs for Paget’s Hypophosphatemia, hypokalemia, hy-
disease or multiple myeloma. pomagnesemia, hypocalcemia occur
Storage • Store parenteral form at more frequently with higher dosages.
room temperature. • Reconstituted vial Anemia, hypertension, tachycardia, atrial
Canadian trade name Non-Crushable Drug High Alert drug
906 panitumumab
fi­ brillation, drowsiness occur more fre- USES
quently with 90-mg doses. GI hemor- Treatment of wild-type RAS metastatic
rhage occurs rarely. colorectal cancer either as first-line ther-
apy in combination with FOLFOX or as
NURSING CONSIDERATIONS
monotherapy following disease progres-
BASELINE ASSESSMENT sion after prior treatment with fluoro-
Obtain CBC, serum calcium, ionized pyrimidine-, oxaliplatin-, or irinotecan-
calcium, magnesium, phosphate; renal based regimens.
function test level prior to therapy. Deter-
mine hydration status.
PRECAUTIONS
Contraindications: Hypersensitivity to pa-
INTERVENTION/EVALUATION nitumumab. Cautions: Interstitial pneu-
Monitor serum calcium, ionized calcium, monitis, pulmonary fibrosis, pulmonary
potassium, magnesium, creatinine, CBC. infiltrates, renal impairment, baseline elec-
Provide adequate hydration; assess over- trolyte imbalance. Not indicated in pts with
hydration. Monitor I&O carefully; assess RAS-mutant metastatic colorectal cancer or
lungs for crackles, dependent body parts for whom RAS mutation status is unknown.
for edema. Monitor B/P, temperature,
pulse. Assess catheter site for redness, ACTION
swelling, pain. Monitor food intake, daily Binds specifically to epidermal growth
pattern of bowel activity, stool consis- factor receptor (EGFR) and competitively
tency. Be alert for potential GI hemor- inhibits binding of epidermal growth
rhage with 90-mg dosage. factor. Blocks activation of intracellular
tyrosine kinase. Therapeutic Effect:
PATIENT/FAMILY TEACHING Inhibits tumor cell growth, survival, and
• Report symptoms of low blood cal- proliferation.
cium levels, including confusion, muscle
P twitching/cramps, numbness, seizures, PHARMACOKINETICS
tingling, jaw pain. • Immediately report Clearance varies by body weight, gender,
GI bleeding. tumor burden. Half-life: 3–10 days.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: May cause fetal
panitumumab harm. May impair fertility. May decrease
fetal body weight, increase risk of skel-
pan-i-toom-ue-mab etal fetal abnormalities. Use effective con-
(Vectibix) traception during and for at least 6 mos
j BLACK BOX ALERT j90% of pts after treatment. Breastfeeding not recom-
experience dermatologic toxicities mended. Children: Safety and efficacy
(dermatitis acneiform, pruritus, ery- not established. Elderly: No age-related
thema, rash, skin exfoliation, skin
fissures, abscess). Severe infusion precautions noted.
reactions (anaphylaxis, bronchos-
pasm, fever, chills, hypotension), INTERACTIONS
fatal reactions have occurred. DRUG: None significant. HERBAL: None
significant. FOOD: None known. LAB
uCLASSIFICATION VALUES: May decrease serum magne-
PHARMACOTHERAPEUTIC: Epider- sium, calcium.
mal growth factor receptor (EGFR)
inhibitor, monoclonal antibody. AVAILABILITY (Rx)
CLINICAL: Antineoplastic. Injection Solution: 20 mg/mL vial (5-mL,
20-mL vials).

underlined – top prescribed drug


panitumumab 907

ADMINISTRATION/HANDLING improved to better than Grade 3. Then,


IV reduce dose as follows: First occurrence
of CTCAE Grade 3: Resume at same
b ALERT c Do not give by IV push or dose. Second occurrence of CTCAE
bolus. Use low protein-binding 0.2- or Grade 3: Reduce dose to 80% of ini-
0.22-micron in-line filter. Flush IV line tial dose. Third occurrence of CTCAE
before and after chemotherapy adminis- Grade 3: Reduce dose to 60% of initial
tration with 0.9% NaCl. dose. Fourth occurrence of CTCAE
Reconstitution • Dilute in 100–150 Grade 3: Permanently discontinue.
mL 0.9% NaCl to provide concentration
of 10 mg/mL or less. • Do not shake Dosage in Renal/Hepatic Impairment
solution. Invert gently to mix. • Discard No dose adjustment.
any unused portion.
SIDE EFFECTS
Rate of administration • Give as IV
infusion over 60 min. • Infuse doses Common (65%–57%): Erythema, acne-
greater than 1,000 mg over 90 min. iform dermatitis, pruritus. Frequent
Storage • Refrigerate vials. • After (26%–20%): Fatigue, abdominal pain,
dilution, solution may be stored for up to skin exfoliation, paronychia (soft tissue
6 hrs at room temperature, up to 24 hrs infection around nailbed), nausea, rash,
if refrigerated. • Discard if discolored, diarrhea, constipation, skin fissures.
but solution may contain visible, translu- Occasional (19%–10%): Vomiting, acne,
cent-to-white particulates (will be re- cough, peripheral edema, dry skin. Rare
moved by in-line filter). (7%–2%): Stomatitis, mucosal inflam-
mation, eyelash growth, conjunctivitis,
IV INCOMPATIBILITIES increased lacrimation.
Do not mix with dextrose solutions or
ADVERSE EFFECTS/TOXIC
any other medications.
REACTIONS P
INDICATIONS/ROUTES/DOSAGE Pulmonary fibrosis, severe dermatologic
b ALERT c Stop infusion immediately toxicity (complicated by infectious se-
in pts experiencing severe infusion quelae) occur rarely. Severe infusion
­reactions. reactions manifested as bronchospasm,
fever, chills, hypotension occur rarely.
Metastatic Colorectal Cancer Hypomagnesemia occurs in 39% of pts.
IV infusion: ADULTS, ELDERLY: 6 mg/ Life-threatening and/or fatal bullous
kg once q14 days as a single agent or in fasciitis, abscess, sepsis were reported.
combination with FOLFOX (fluorouracil, Severe dehydration and diarrhea may
leucovorin and oxaliplatin). Continue increase risk of acute renal failure. Ex-
until disease progression or unaccept- posure to sunlight may exacerbate skin
able toxicity. toxicities. May cause ocular toxicities
including keratitis, ulcerative keratitis,
Dose Modification corneal ulceration.
Infusion Reactions
Mild to moderate reactions: Reduce NURSING CONSIDERATIONS
infusion rate by 50% for remainder of in-
BASELINE ASSESSMENT
fusion. Severe reactions: Discontinue
infusion. Depending on severity, consider Assess serum magnesium, calcium prior
permanent discontinuation. to therapy, periodically during therapy,
and for 8 wks after completion of therapy.
Skin Toxicity Assess KRAS mutational status in colorec-
For all CTCAE Grade 3 skin toxicities, tal tumors and confirm the absence of a
withhold treatment for 1–2 doses until RAS mutation.
Canadian trade name Non-Crushable Drug High Alert drug
908 panobinostat
INTERVENTION/EVALUATION USES
Assess for skin, ocular, mucosal, pulmo- Used in combination with bortezomib
nary toxicity; report effects. Median time and dexamethasone for treatment of pts
to development of skin/ocular toxicity is with multiple myeloma who have re-
14–15 days; resolution after last dosing ceived at least 2 prior regimens, includ-
is 84 days. Monitor serum electrolytes ing bortezomib and an immunomodula-
for hypomagnesemia, hypocalcemia. Of- tory agent.
fer antiemetic if nausea/vomiting occurs.
Monitor daily pattern of bowel activity, PRECAUTIONS
stool consistency. Contraindications: Hypersensitivity to pan-
PATIENT/FAMILY TEACHING obinostat. Cautions: Congenital long QT
syndrome, concurrent medications that
• Do not have immunizations without prolong QT interval, electrolyte abnormal-
physician’s approval (drug lowers resis- ities (hypokalemia, hypomagnesemia),
tance). • Avoid contact with those who renal impairment. Not recommended in
have recently received a live virus vac- pts with recent MI or unstable angina, se-
cine. • Avoid crowds, those with infec- vere hepatic impairment. Concurrent use
tion. • There is a potential risk for of strong CYP3A inhibitors and/or CYP3A
development of fetal abnormalities if preg- inducers, CYP2D6 substrates not recom-
nancy occurs; take measures to prevent mended. Preexisting myelosuppression.
pregnancy. • Report skin reactions, in- Avoid use in pts with active infection.
cluding rash, sloughing, blisters, ero-
sions. • Report difficulty breathing, fever ACTION
with cough, lung pain; may indicate life- Inhibits enzymatic activity of histone
threatening lung inflammation. • Limit deacetylase. Increases acetylation of his-
sun, UV exposure. Wear protective sun- tone proteins, resulting in cell cycle arrest
screen, hats, and clothing while outdoors. and/or cellular death (apoptosis). Thera-
P peutic Effect: Inhibits tumor growth and
metastasis. Promotes tumor cell death.
panobinostat PHARMACOKINETICS
pan-oh-bin-oh-stat Widely distributed. Extensively metabo-
(Farydak) lized. Protein binding: 90%. Peak plasma
j BLACK BOX ALERT jSevere concentration: 2 hrs. Excreted in feces
cases of diarrhea reported in 25% (44%–77%), urine (29%–51%). Half-
of pts. If diarrhea occurs, interrupt life: 37 hrs.
treatment, initiate antidiarrheal ther-
apy, and then reduce or discontinue LIFESPAN CONSIDERATIONS
treatment. Severe and/or fatal cases
of cardiac arrhythmias, cardiac Pregnancy/Lactation: Avoid preg-
ischemic events, ECG changes may nancy; may cause fetal harm/malforma-
occur. Electrolyte abnormalities may tions. Females of reproductive potential
increase risk of arrhythmias. Obtain should use effective contraception dur-
ECG, serum electrolytes at baseline
and monitor during treatment. ing treatment and up to 1 mo after dis-
Do not confuse panobinostat continuation. Unknown if distributed in
with febuxostat or pentostatin. breast milk. Males: Males should use
condoms during sexual activity during
uCLASSIFICATION treatment and up to 3 mos after discon-
PHARMACOTHERAPEUTIC: Histone tinuation. Children: Safety and efficacy
deacetylase (HDAC) inhibitor. CLINI- not established. Elderly: May have in-
CAL: Antineoplastic. creased risk of adverse effects (e.g., car-
diac/GI/hematologic toxicities).
underlined – top prescribed drug
panobinostat 909

INTERACTIONS dose of dexamethasone: 20 mg orally/


DRUG: Strong CYP3A inhibitors day on a full stomach per dosing schedule.
(e.g., clarithromycin, ketoconazole, Dosing Schedule for Cycles 1–8 of 21-Day
ritonavir) may increase concentra- Cycle
tion/effect. Strong CYP3A inducers Wk 1: Panobinostat: days 1, 3, 5. Bort-
(e.g., carBAMazepine, rifAMPin) ezomib: days 1, 4. Dexamethasone:
may decrease concentration/effect. days 1, 2, 4, 5. Wk 2: Panobinostat:
May increase concentration/effects of days 8, 10, 12. Bortezomib: days 8,
CYP2D6 substrates (e.g., meto- 11. Dexamethasone: days 8, 9, 11, 12.
prolol, venlafaxine). Amiodarone, Wk 3: Rest period (all 3 drugs).
azithromycin, ceritinib, haloperi-
dol, moxifloxacin may increase risk of Dosing Schedule for Cycles 9–16 of 21-
QT interval prolongation. May decrease Day Cycle
the therapeutic effect; increase adverse Wk 1: Panobinostat: days 1, 3, 5. Bort-
effects of vaccines (live). HERBAL: St. ezomib: day 1 only. Dexamethasone: days
John’s wort may decrease concentra- 1, 2. Wk 2: Panobinostat: days 8, 10,
tion/effect. FOOD: High-fat meals may 12. Bortezomib: day 8 only. Dexametha-
delay absorption. Grapefruit products, sone: days 8, 9. Wk 3: Rest period (all
star fruit may increase concentration/ 3 drugs).
effect. LAB VALUES: May decrease Hct,
Hgb, leukocytes, lymphocytes, neutro- Dose Reduction for Adverse Events
phils, platelets; serum albumin, calcium, If reduction required, reduce panobino-
potassium, sodium. May increase serum stat in increments of 5 mg. If the reduced
bilirubin, creatinine, magnesium. May dose is less than 10 mg 3 times/wk, dis-
increase or decrease phosphate. continue treatment. Keep same schedule
(21-day cycle) when dose reduced.
AVAILABILITY (Rx)
Dose Modification for Clinical Toxicities P
Capsules: 10 mg, 15 mg, 20 mg. Based on Common Terminology Criteria
ADMINISTRATION/HANDLING for Adverse Events (CTCAE).
PO Thrombocytopenia
• May give without regard to food; avoid Grade 3: No dose adjustment. (Bort-
grapefruit products (dexamethasone ezomib): No dose adjustment. Grade
should be given with food to decrease GI 3 with bleeding/Grade 4: Interrupt
upset). • Administer capsule whole; do treatment until platelet count 50,000
not break, cut, crush, or open. • If vomit- cells/mm3 or greater, then resume at re-
ing occurs after dosing, do not readminis- duced dose. (Bortezomib): Interrupt
ter dose; give dose at next scheduled time. bortezomib until platelet count 75,000
cells/mm3 or greater. If only 1 dose was
INDICATIONS/ROUTES/DOSAGE held prior to resolution of platelet count,
Multiple Myeloma resume bortezomib at same dose. If more
PO: ADULTS, ELDERLY: 20 mg once ev- than 2 doses were held consecutively, re-
ery other day for 3 doses/wk during wk sume bortezomib at reduced dose.
1 and 2 of each 21-day cycle for up to 8
cycles, in combination with bortezomib Neutropenia
and dexamethasone. Consider continuing Grade 3: No dose adjustment. (Bortezo-
treatment for additional 8 cycles based mib): No dose adjustment. Two or more
on tolerability. Total duration: Up to 16 occurrences of Grade 3: Interrupt
cycles (48 wks). Recommended dose treatment until ANC 1,000 cells/mm3 or
of bortezomib: 1.3 mg/m2 as injection/ greater, then resume at same dose. (Bort-
day per dosing schedule. Recommended ezomib): No dose adjustment. Grade

Canadian trade name Non-Crushable Drug High Alert drug


910 panobinostat
3 with febrile neutropenia/Grade Dosage in Hepatic Impairment
4: Interrupt treatment until febrile neutro- PO: ADULTS, ELDERLY: Mild impair-
penia resolves and ANC is 1,000 cells/mm3 ment: 15 mg per dosing schedule. Mod-
or greater, then resume at reduced dose. erate ­impairment: 10 mg per dosing
(Bortezomib): Interrupt bortezomib schedule. Severe impairment: Treat-
until febrile neutropenia resolves and ANC ment not recommended.
is 1,000 cells/mm3 or greater. If only 1
dose was held prior resolution of platelet SIDE EFFECTS
count, resume bortezomib at same dose. If Frequent (60%–2%): Fatigue, asthenia, leth-
more than 2 doses were held consecutively, argy, diarrhea, nausea, peripheral edema,
resume bortezomib at reduced dose. decreased appetite, vomiting, pyrexia. Oc-
casional (12%): Decreased weight.
Anemia
Grade 3: Interrupt panobinostat until ADVERSE EFFECTS/TOXIC
Hgb greater than or equal to 10 g/dL, REACTIONS
then resume at reduced dose. (Bortezo- Anemia, leukopenia, neutropenia,
mib): Not specified. thrombocytopenia are expected re-
sponses to therapy. Diarrhea occurred
Diarrhea in 68% of pts. Severe cases of diarrhea
Grade 2: Interrupt treatment until occurred in 25% of pts. Cardiac toxici-
resolved, then resume at same dose. ties such as cardiac ischemic events, ST-
(Bortezomib): Consider interruption segment depression, T-wave abnormali-
of bortezomib until resolved, then resume ties were reported. Cardiac arrhythmias
at same dose. Grade 3 or hospitaliza- including atrial fibrillation, atrial flutter,
tion/administration of IV fluids: In- bradycardia, SVT, atrial/ventricular/sinus
terrupt until resolved, then resume at tachycardia occurred in 12% of pts. Se-
reduced dose. (Bortezomib): Interrupt vere thrombocytopenia may increase risk
P until resolved, then resume bortezomib of fatal hemorrhage. Infectious processes
at reduced dose. Grade 4: Permanently such as bacterial infections, invasive fun-
discontinue panobinostat and bortezomib. gal infections, pneumonia, sepsis, viral
infections were reported. Severe and/or
Nausea/Vomiting fatal infections occurred in 31% of pts.
Grade 3 or 4: Interrupt until resolved,
then resume at reduced dose. (Bortezo- NURSING CONSIDERATIONS
mib): Not specified.
BASELINE ASSESSMENT
Other Toxicities (Other CTCAE Grades) Obtain CBC, BMP, LFT; serum magnesium,
Any Grade 2 recurrence, any other phosphate; ECG, vital signs. Correct elec-
Grade 3 or 4: Interrupt until resolved to trolyte imbalances prior to each cycle.
Grade 1 or 0, then resume at reduced dose. Verify platelet count is at least 100,000
(Bortezomib): Not specified. Any other cells/mm3, ANC is 1,500 cells/mm3, QTc
Grade 3 or 4 recurrence: Consider interval is less than 450 msec on ECG
further dose reduction once resolved to prior to each cycle. Verify pregnancy sta-
Grade 1 or 0. tus. Assess hydration status, usual stool
characteristics. Question history if acute
Concomitant Use of Strong CYP3A MI, unstable angina, arrhythmia. Screen
Inhibitors for active infection.
PO: ADULTS, ELDERLY: 10 mg per dosing
schedule. INTERVENTION/EVALUATION
Monitor CBC, BMP; serum magnesium,
Dosage in Renal Impairment phosphate wkly; LFT as indicated; vital
No dose adjustment. signs. Monitor ECG periodically. If QTc
underlined – top prescribed drug
pantoprazole 911
interval increases to greater than 480 uCLASSIFICATION
msec on ECG, interrupt treatment and PHARMACOTHERAPEUTIC: Benzi-
correct any electrolyte abnormalities. If midazole. CLINICAL: Proton pump
QT p­ rolongation does not resolve, per- inhibitor.
manently discontinue treatment. Initiate
medical management for nausea, vomit-
ing, diarrhea prior to any interruption or USES
dose reduction. Consider blood transfu- PO: Treatment, maintenance of healing
sion in pts with severe anemia, thrombo- of erosive esophagitis associated with
cytopenia. Diligently monitor daily pat- gastroesophageal reflux disease (GERD)
tern bowel activity, stool consistency. Start and reduction of relapse rate of heart-
antidiarrheal therapy at first sign of loose burn symptoms in GERD. Treatment of
stool/diarrhea. Obtain 2D cardiac echo- hypersecretory conditions including
cardiogram, ECG if cardiac decompensa- Zollinger-Ellison syndrome. IV: Short-
tion is suspected. Monitor for infection. term treatment of erosive esophagitis
PATIENT/FAMILY TEACHING associated with GERD, treatment of
hypersecretory conditions. OFF-LABEL:
• Blood levels will be monitored regu- Peptic ulcer disease, active ulcer bleed-
larly. • Treatment may cause fetal ing (injection), adjunct in treatment of
harm. Women of childbearing potential H. pylori, stress ulcer prophylaxis in
should use effective contraception during critically ill pts.
treatment and up to 1 mo after final dose.
Immediately report suspected pregnancy. PRECAUTIONS
Do not breastfeed. • Therapy may re- Contraindications: Hypersensitivity to pan­
duce fertility in both female and male toprazole, other proton pump inhibitors
pts. • Male pts must use condoms dur- (e.g., omeprazole). Cautions: May in-
ing sexual activity. • Report liver prob- crease risk of fractures, GI infections.
lems such as upper abdominal pain, P
bruising, dark or amber-colored urine, ACTION
nausea, vomiting, or yellowing of the skin Irreversibly binds to, inhibits hydrogen-
or eyes; heart problems such as chest potassium adenosine triphosphate, an
tightness, dizziness, fainting, palpitations, enzyme on surface of gastric parietal
shortness of breath; kidney problems cells. Inhibits hydrogen ion transport into
such as dark-colored urine, decreased gastric lumen. Therapeutic Effect: In-
urine output, extremity swelling, flank creases gastric pH, reduces gastric acid
pain; skin changes such as rash, red- production.
ness. • Report mouth ulceration, jaw
pain. • Swallow capsules whole; do not PHARMACOKINETICS
chew, crush, cut, or open capsules.
Route Onset Peak Duration
• Treatment may increase risk of bleed-
ing, nosebleeds. • Drink plenty of PO N/A N/A 24 hrs
­fluids. • Report the first signs of ab- Well absorbed from GI tract. Protein
dominal cramping, loose stool, diarrhea. binding: 98% (primarily albumin). Pri-
marily distributed into gastric parietal
cells. Metabolized in liver. Primarily ex-
pantoprazole creted in urine. Not removed by hemodi-
alysis. Half-life: 1 hr.
pan-toe-pra-zole
(Pantoloc , Protonix, Tecta ) LIFESPAN CONSIDERATIONS
Do not confuse pantoprazole Pregnancy/Lactation: Unknown if
with ARIPiprazole. drug crosses placenta or is distributed
Canadian trade name Non-Crushable Drug High Alert drug
912 pantoprazole
in breast milk. Children: Safety and IV INCOMPATIBILITIES
efficacy not established. Elderly: No
­ DOBUTamine.
age-related precautions noted.
IV COMPATIBILITIES
INTERACTIONS DOPamine, EPINEPHrine, furosemide
DRUG: May decrease concentration/ (Lasix), insulin (regular), potassium
effect of acalabrutinib, cefurox- chloride, vasopressin.
ime, erlotinib, neratinib, pazo-
panib. Strong CYP2C19 inducers INDICATIONS/ROUTES/DOSAGE
(e.g., FLUoxetine), strong CYP3A4 Erosive Esophagitis (Treatment)
inducers (e.g., carBAMazepine, PO: ADULTS, ELDERLY: 40 mg/day for up to
phenytoin, rifAMPin) may decrease 8 wks. If not healed after 8 wks, may con-
concentration/effect. HERBAL: None tinue an additional 8 wks. CHILDREN 5 YRS
significant. FOOD: None known. LAB AND OLDER (WEIGHING 40 KG OR MORE): 40
VALUES: May increase serum creati- mg/day for up to 8 wks. (WEIGHING 15–39
nine, cholesterol, uric acid, glucose, KG): 20 mg/day for up to 8 wks.
lipoprotein, ALT. IV: ADULTS, ELDERLY: 40 mg/day for
7–10 days.
AVAILABILITY (Rx)
Maintenance of Healing of Erosive
Granules for Suspension: 40 mg/packet. Esophagitis
Injection, Powder for Reconstitution: (Pro- PO: ADULTS, ELDERLY: 40 mg once daily.
tonix): 40 mg.
Hypersecretory Conditions
Tablets, Delayed-Release: (Protonix):
PO: ADULTS, ELDERLY: Initially, 80 mg
20 mg, 40 mg.
twice daily. May titrate upward early in
ADMINISTRATION/HANDLING therapy. Maximum: 240 mg/day (as ei-
ther 80 mg three times daily or 120 mg
P IV twice daily).
Reconstitution • Mix 40-mg vial with IV: ADULTS, ELDERLY: 80 mg twice daily.
10 mL 0.9% NaCl injection. • May be May increase to 80 mg q8h.
further diluted with 100 mL D5W, 0.9% Prevention of Rebleeding in Peptic Ulcer
NaCl. Bleed (Unlabeled)
Rate of administration • Infuse 10 IV: ADULTS, ELDERLY: 80 mg followed
mL solution over at least 2 min. • In- by 8 mg/hr infusion for 72 hrs or 80 mg
fuse 100 mL solution over at least 15 then 40 mg q12h for 72 hrs.
min. • Flush IV line after administra-
tion. Dosage in Renal/Hepatic Impairment
Storage • Store undiluted vials at No dose adjustment.
room temperature. • Once diluted with SIDE EFFECTS
10 mL 0.9% NaCl, stable for 96 hrs at
room temperature; when further diluted Rare (less than 2%): Diarrhea, headache,
with 100 mL, stable for 96 hrs at room dizziness, pruritus, rash.
temperature. ADVERSE EFFECTS/TOXIC
PO
REACTIONS
• May be given without regard to food. Hyperglycemia occurs rarely. May increase
Best given before breakfast. • Do not risk of C. difficile–associated diarrhea.
break, crush, dissolve, or divide tablets; NURSING CONSIDERATIONS
give whole. • Administer oral suspen-
sion only in apple juice or applesauce. BASELINE ASSESSMENT
Best taken 30 min before a meal. Question history of GI disease, ulcers, GERD.

underlined – top prescribed drug


PARoxetine 913
INTERVENTION/EVALUATION injurious behavior, treatment of depres-
Evaluate for therapeutic response (re- sion and OCD in children.
lief of GI symptoms). Question if GI
­discomfort, nausea occur. Monitor for PRECAUTIONS
abdominal pain, diarrhea (with or with- Contraindications: Hypersensitivity to PAR-
out fever). oxetine. Concurrent use of MAOIs with
or within 14 days of MAOIs intended to
PATIENT/FAMILY TEACHING treat psychiatric disorders, initiation in pts
• Report abdominal pain, diarrhea treated with linezolid or methylene blue;
(with or without fever) that does not concomitant use with thioridazine, pimo-
resolve; may indicate colon infec- zide. Brisdelle: Pregnancy. Cautions:
tion. • Avoid alcohol. • Swallow tab- History of seizures, renal/hepatic impair-
lets whole; do not chew, crush, dissolve, ment, pts with suicidal tendencies, elderly
or divide. • Best if given before break- pts, narrow-angle glaucoma; avoid use in
fast. May give without regard to food. first trimester of pregnancy, alcohol use.
ACTION
PARoxetine Selectively blocks uptake of neurotransmit-
ter serotonin at CNS neuronal presynaptic
par-ox-e-teen membranes, increasing its availability at
(Brisdelle, Paxil, Paxil CR, Pexeva) postsynaptic receptor sites. Therapeutic
Effect: Relieves depression, reduces obses-
j BLACK BOX ALERT jIncreased sive-compulsive behavior, decreases anxiety.
risk of suicidal thinking and behav-
ior in children, adolescents, young
adults 18–24 yrs with major depres- PHARMACOKINETICS
sive disorder, other psychiatric Well absorbed from GI tract. Protein bind-
disorders. ing: 95%. Widely distributed. Metabolized
Do not confuse PARoxetine in liver. Excreted in urine. Not removed by P
with piroxicam, FLUoxetine or hemodialysis. Half-life: 24 hrs.
pyridoxine, or Paxil with Doxil,
Plavix, PROzac, or Taxol. LIFESPAN CONSIDERATIONS
uCLASSIFICATION Pregnancy/Lactation: May impair
reproductive function. Not distributed in
PHARMACOTHERAPEUTIC: Selective breast milk. May increase risk of congen-
serotonin reuptake inhibitor (SSRI). ital malformations. Children: Safety and
CLINICAL: Antidepressant, antiob- efficacy not established. Elderly: Age-
sessive-compulsive, antianxiety. related renal impairment may require
dosage adjustment. Use caution.
USES INTERACTIONS
Treatment of major depressive disorder DRUG: Alcohol may increase adverse
(MDD). Treatment of panic disorder, effects. Lithium, MAOIs (e.g., phenel-
obsessive-compulsive disorder (OCD). zine, selegiline) may increase the sero-
Treatment of social anxiety disorder tonergic effect. May increase antiplatelet
(SAD), generalized anxiety disorder effect of NSAIDs (e.g., ibuprofen,
(GAD), premenstrual dysphoric disorder ketorolac, naproxen). May decrease
(PMDD), post-traumatic stress disorder concentration/effect of tamoxifen. May
(PTSD). Brisdelle: Treatment of mod- increase adverse effects of tricyclic an-
erate to severe vasomotor symptoms tidepressants (e.g., amitriptyline).
associated with menopause. OFF-LABEL: HERBAL: Glucosamine, herbals with
Social anxiety disorder in children, self- anticoagulant/antiplatelet properties

Canadian trade name Non-Crushable Drug High Alert drug


914 PARoxetine
(e.g., garlic, ginger, ginkgo biloba) increase by 12.5 mg/day at wkly intervals.
may increase effect. FOOD: None known. Maximum: 75 mg/day.
LAB VALUES: May decrease Hgb, Hct,
Social Anxiety Disorder (SAD)
WBC count.
PO: (Immediate-Release): ADULTS:
AVAILABILITY (Rx) Initially, 10 mg/day. May increase by 10
Capsules: (Brisdelle): 7.5 mg. Oral Sus- mg/day at intervals of more than 1 wk.
pension: (Paxil): 10 mg/5 mL. Tablets: Maximum: 60 mg/day.
(Paxil, Pexeva): 10 mg, 20 mg, 30 mg, PO: (Controlled-Release): ADULTS, EL-
40 mg. DERLY: Initially, 12.5 mg once daily. May
increase by 12.5 mg/day at wkly intervals.
Tablets, Controlled-Release: (Paxil CR):
Maximum: 37.5 mg/day.
12.5 mg, 25 mg, 37.5 mg.
Post-traumatic Stress Disorder (PTSD)
ADMINISTRATION/HANDLING PO: (Immediate-Release): ADULTS: Ini­
PO tially, 20 mg/day. May increase by 10–20
• May give without regard to mg/day at intervals of more than 1 wk.
food. • Give with food, milk if GI dis- Maximum: 60 mg/day.
tress occurs. • Scored tablet may be
Premenstrual Dysphoric Disorder (PMDD)
crushed. • Do not crush, break, dis-
PO: (Controlled-Release): ADULTS: Ini-
solve, or divide controlled-release tablets.
tially, 12.5 mg/day. May increase by 12.5 mg
INDICATIONS/ROUTES/DOSAGE at wkly intervals. Maximum: 50 mg/day.
Depression Vasomotor Symptoms
PO: (Immediate-Release): ADULTS: Ini­ PO: ADULTS: (Brisdelle): 7.5 mg once
tially, 10–20 mg/day. May increase by daily at bedtime.
­10–20 mg/day at intervals of more than 1
wk. Maximum: 50 mg/day. Usual Elderly Dosage
P PO: (Controlled-Release): ADULTS: Ini­ PO: Initially, 10 mg/day. May increase by
tially, 25 mg/day. May increase by 12.5 mg/ 10 mg/day at intervals of more than 1 wk.
day at intervals of more than 1 wk. Maxi- Maximum: 40 mg/day.
mum: 62.5 mg/day. PO: (Controlled-Release): Initially, 12.5
mg/day. May increase by 12.5 mg/day at in-
Generalized Anxiety Disorder (GAD) tervals of more than 1 wk. Maximum: 50
PO: (Immediate-Release): ADULTS: Ini­ mg/day (37.5 mg for SAD).
tially, 10 mg/day. May increase by 10 mg/
Dosage Renal/Hepatic Impairment
day at intervals of more than 1 wk. Range:
CrCl less than 30 mL/min, severe
20–50 mg/day.
hepatic impairment: (Immediate-­
Obsessive-Compulsive Disorder (OCD) Release): Initially, 10 mg/day. May in-
PO: (Immediate-Release): ADULTS: crease by 10 mg/dose at wkly intervals.
Initially, 20 mg/day. May increase by 10 Maximum: 40 mg/day. (Extended-
mg/day at intervals of more than 1 wk. Release): Initially, 12.5 mg/day. May in-
Recommended dose: 40–60 mg/day. crease by 12.5 mg/day at wkly intervals.
Maximum: 50 mg/day. (Brisdelle): No
Panic Disorder dosage adjustment.
PO: (Immediate-Release): ADULTS:
Initially, 10 mg/day. May increase by 10 SIDE EFFECTS
mg/day at intervals of more than 1 wk. Frequent (26%–8%): Nausea, drowsiness,
Usual dose: 20–40 mg/day. Maximum: headache, dry mouth, asthenia, constipa-
60 mg/day. tion, dizziness, insomnia, diarrhea, diapho-
PO: (Controlled-Release): ADULTS, EL- resis, tremor. Occasional (6%–3%): De-
DERLY: Initially, 12.5 mg once daily. May creased appetite, respiratory disturbance
underlined – top prescribed drug
PAZOPanib 915
(e.g., increased cough), anxiety, flatulence, uCLASSIFICATION
paresthesia, yawning, decreased libido, PHARMACOTHERAPEUTIC: Vascular
sexual dysfunction, abdominal discomfort. endothelial growth factor (VEGF)
Rare: Palpitations, vomiting, blurred vi- inhibitor. Tyrosine kinase inhibitor.
sion, altered taste, confusion. CLINICAL: Antineoplastic.
ADVERSE EFFECTS/TOXIC
REACTIONS USES
Hyponatremia, seizures have been re- Treatment of advanced renal cell carci-
ported. Serotonin syndrome (agitation, noma (RCC), advanced soft-tissue sar-
confusion, diaphoresis, hallucinations, coma (STS) (in pts previously treated
hyperreflexia) occurs rarely. with chemotherapy). OFF-LABEL: Ad-
vanced thyroid cancer.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT PRECAUTIONS
Obtain baseline LFT. Assess appearance, Contraindications: Hypersensitivity to PA-
behavior, speech pattern, level of inter- ZOPanib. Cautions: Avoid use of strong
est, mood. CYP3A4 inhibitors (e.g., clarithromycin,
ketoconazole) or CYP3A inducers (carBA-
INTERVENTION/EVALUATION Mazepine, rifAMPin) and grapefruit prod-
For pts on long-term therapy, CBC, LFT, ucts. Cautious use in pts with increased
renal function test should be performed risk or history of arterial thrombotic
periodically. Assess mental status for events (e.g., angina, MI, ischemic stroke),
depression, suicidal ideation (esp. at be- QT prolongation, hypokalemia, hypomag-
ginning of therapy or change in dosage), nesemia, hypertension, severe hepatic im-
anxiety, social functioning, panic attacks. pairment, history of hemoptysis, cerebral
Assess appearance, behavior, speech pat- hemorrhage or significant GI hemorrhage.
tern, level of interest, mood. Concomitant use of medications that may P
prolong QT interval not recommended.
PATIENT/FAMILY TEACHING
• Avoid alcohol, St. John’s ACTION
wort. • Therapeutic effect may be noted Inhibits cell surface vascular endothelial
within 1–4 wks. • Do not abruptly dis- growth factor (VEGF) receptors. Thera-
continue medication. • Avoid tasks that peutic Effect: Inhibits angiogenesis,
require alertness, motor skills until re- blocks tumor growth.
sponse to drug is established. • May
impair reproductive function. • Report PHARMACOKINETICS
suspected pregnancy. • Report worsen- Peak concentration occurs 2–4 hrs fol-
ing depression, suicidal ideation, un- lowing oral administration. Metabolized
usual changes in behavior. in liver. Protein binding: greater than
99%. Excreted in feces (60%), urine
(23%). Half-life: 31 hrs.
PAZOPanib
LIFESPAN CONSIDERATIONS
paz-oh-pa-nib Pregnancy/Lactation: May cause fetal
(Votrient) harm. Unknown if distributed in breast
j BLACK BOX ALERT jSevere, milk. Children: Safety and efficacy not
fatal hepatotoxicity has been established. Elderly: No age-related pre-
observed. cautions noted.

Canadian trade name Non-Crushable Drug High Alert drug


916 PAZOPanib

INTERACTIONS Dosage in Renal Impairment


DRUG: Histamine H2 antagonists No dose adjustment.
(e.g., famotidine, ranitidine), pro- Dosage in Hepatic Impairment
ton pump inhibitors (e.g., omepra- Mild impairment: No dose adjustment.
zole, pantoprazole) may decrease Moderate impairment: Reduce dose
concentration/effect. QT interval–pro- to 200 mg/day. Severe impairment:
longing medications (e.g., amio- Not recommended.
darone, citalopram, haloperidol,
ondansetron) may prolong QT interval. SIDE EFFECTS
CYP3A4 inhibitors (e.g., clarithro- Frequent (52%–19%): Diarrhea, hyper-
mycin, ketoconazole, ritonavir) tension, hair color changes, nausea,
may increase concentration. CYP3A4 fatigue, anorexia, vomiting. Occasional
inducers (e.g., carBAMazepine, phe- (14%–10%): Asthenia, abdominal pain,
nytoin, rifAMPin) may decrease con- headache. Rare (less than 10%): Alope-
centration. May decrease the therapeutic cia, chest pain, altered taste, dyspepsia,
effect; increase adverse effects of vac- proteinuria, rash, decreased weight.
cines (live). HERBAL: St. John’s wort
decreases concentration. FOOD: Food ADVERSE EFFECTS/TOXIC
may increase concentration. Grapefruit REACTIONS
products may increase concentration, Hepatotoxicity, manifested as increase
potential for torsades de pointes, my- in serum bilirubin, ALT, AST, has been
elotoxicity. LAB VALUES: May decrease observed and may be fatal. Hemorrhagic
serum phosphorus, sodium, magnesium, events (hematuria, epistaxis, hemoptysis,
glucose, WBC count. May increase serum GI bleeding or perforation, intracranial
ALT, AST. hemorrhage) have been noted and may
AVAILABILITY (Rx) be fatal. Hypertension (B/P greater than
P 150/100 mm Hg) is common (47% of
Tablets: 200 mg. pts), usually occurring early in the first
18 wks of treatment. Hypothyroidism
ADMINISTRATION/HANDLING has been reported occasionally. Arterial
PO thrombotic events (MI, CVA), QT pro-
• Give at least 1 hr before or 2 hrs after longation, torsades de pointes have been
ingestion of food. • Give tablets whole; seen rarely.
do not break, crush, dissolve, or divide.
NURSING CONSIDERATIONS
INDICATIONS/ROUTES/DOSAGE
BASELINE ASSESSMENT
Renal Cell Carcinoma, Soft-Tissue
Sarcoma Obtain baseline ECG, CBC, serum chem-
PO: ADULTS, ELDERLY: 800 mg once istries, LFT. Assess medical history, esp.
daily. If concomitant CYP3A4 inhibitor hepatic impairment. Question history of
cannot be discontinued, reduce initial hepatic impairment, arterial or venous
dose to 400 mg/day. thromboembolism, GI bleeding. Receive
full medication history and screen for
Dose Adjustment for Toxicity interactions.
Prior to dose reduction, temporarily dis-
INTERVENTION/EVALUATION
continue therapy if 24-hr urine protein
3 g or more (or for other toxicities). Monitor B/P, LFT periodically for eleva-
Initial dose reduction: Renal cell carci- tions. Monitor CBC, serum chemistries for
noma: 400 mg/day. Soft tissue sarcoma: changes from baseline. Observe for hepa-
600 mg/day. Further dose adjustment: totoxicity (jaundice, dark-colored urine,
200 mg/day. unusual fatigue, right upper quadrant

underlined – top prescribed drug


pegfilgrastim 917
abdominal pain). Observe ECG for QT-in- adolescents weighing less than 45 kg. Do
terval prolongation. Monitor for evidence not administer within 14 days before and
of bleeding, hemorrhage. Monitor daily 24 hrs after cytotoxic chemotherapy.
pattern of bowel activity, stool consistency.
ACTION
PATIENT/FAMILY TEACHING
Stimulates production, maturation, and
• Avoid crowds, those with known infec- activation of neutrophils within bone
tion. • Avoid contact with anyone who marrow. Therapeutic Effect: Increases
recently received live virus vaccine; do phagocytic ability, antibody-dependent
not receive vaccinations. • Swallow destruction; decreases incidence of
tablets whole; do not chew, crush, dis- ­infection.
solve, or divide. • No food should be
taken at least 1 hr before and 2 hrs after PHARMACOKINETICS
dose is taken. • Avoid grapefruit prod- Readily absorbed after SQ administra-
ucts. • Report diarrhea, abdominal tion. Half-life: 15–80 hrs.
pain, yellowing of skin or sclera, discol-
ored urine, fatigue. • Report bleeding LIFESPAN CONSIDERATIONS
of any kind, esp. bloody stools, nose- Pregnancy/Lactation: Unknown if
bleeds, coughing up blood. • Treat- drug crosses placenta or is distributed
ment may increase risk of heart attack, in breast milk. Children: Safety and ef-
stroke, blood clots, or heart arrhythmias. ficacy not established in children younger
than 12 yrs. Elderly: No age-related
precautions noted.
pegfilgrastim INTERACTIONS
peg-fil-gras-tim DRUG: Pegloticase may decrease effect.
(Neulasta, Neulasta Onpro, Fulphila, HERBAL: None significant. FOOD: None
Udenyca) known. LAB VALUES: May increase se- P
Do not confuse Neulasta with rum LDH, alkaline phosphatase, uric acid.
Lunesta, Neumega, or Neupogen. AVAILABILITY (Rx)
uCLASSIFICATION Injection Solution: (Neulasta): 6 mg/0.6
PHARMACOTHERAPEUTIC: Colony- mL syringe. Prefilled Syringe Kit: (Neu-
stimulating factor. CLINICAL: Hemat- lasta Onpro): 6 mg/0.6 mL; dose delivers
opoietic agent. over 45 min. time period about 27 hrs
after application. Prefilled Syringe: (Ful-
phila, Udenyca): 6 mg/0.6 mL.
USES
Decreases incidence of infection (as mani-
ADMINISTRATION/HANDLING
fested by febrile neutropenia) in cancer pts SQ
receiving myelosuppressive chemotherapy Storage • Store in refrigerator. Warm
associated with febrile neutropenia. To to room temperature prior to administer-
increase survival in pts acutely exposed to ing injection. • Administer to outer up-
myelosuppressive doses of radiation. per arms, abdomen (except within 2
inches of navel), front middle thigh or
PRECAUTIONS upper outer buttocks. Discard if left at
Contraindications: Hypersensitivity to room temperature for more than 48
pegfilgrastim, filgrastim. Cautions: Any hrs. • Protect from light. • Avoid
malignancy with myeloid characteristics, freezing; but if accidentally frozen, may
sickle cell disease. The 6-mg fixed dose allow to thaw in refrigerator before ad-
not to be used in infants, children, or ministration. Discard if freezing takes
Canadian trade name Non-Crushable Drug High Alert drug
918 pegloticase
place a second time. • Discard if dis- from antibody response to growth factors
colored or precipitate forms. occurs rarely. Splenomegaly occurs rarely.
Severe sickle cell crisis reported in pts
On Body Injector (OnPro) with sickle cell disease. Glomerulonephri-
A health care provider must fill the injec- tis, capillary leak syndrome, tumor growth
tor prior to applying to pt’s skin. Apply to stimulatory effect on malignant cells, acute
intact, nonirritated skin on back of arms respiratory distress syndrome may occur.
or abdomen. Delivers pegfilgrastim over
45 min. time period about 27 hrs after NURSING CONSIDERATIONS
application. May apply on same day as
BASELINE ASSESSMENT
chemotherapy. Keep injector at least 4
inches away from electrical equipment. Obtain CBC prior to initiation and routinely
thereafter. Question history of sickle cell
INDICATIONS/ROUTES/DOSAGE disease, glomerulonephritis, splenic disease,
Neutropenia (Chemotherapy-Induced) hypersensitivity reaction to acrylic adhe-
SQ: ADULTS, ELDERLY, CHILDREN 12–17 sive on body (injector uses acrylic adhesive).
YRS, WEIGHING MORE THAN 45 KG: Give as INTERVENTION/EVALUATION
single 6-mg injection once per chemo-
therapy cycle beginning at least 24 hrs Monitor for allergic reactions. Assess for
after completion of chemotherapy. peripheral edema. Assess mucous mem-
b ALERT c Do not administer between branes for evidence of stomatitis, mu-
14 days before and 24 hrs after cytotoxic cositis. Assess muscle strength. Monitor
chemotherapy. Do not use in infants, chil- daily pattern of bowel activity, stool con-
dren, adolescents weighing less than 45 kg. sistency. Adult respiratory distress syn-
drome (ARDS) may occur in septic pts.
Radiation Injury Syndrome
PATIENT/FAMILY TEACHING
Note: Prefilled syringe not designed to give
doses less than 6 mg. Not recommended; • Inform pt of possible side effects, signs/
P symptoms of allergic reaction. • Coun-
use caution to avoid dosing errors.
SQ: ADULTS, ELDERLY, CHILDREN WEIGH- sel pt on importance of compliance with
ING 45 KG OR MORE: 6 mg once wkly for pegfilgrastim treatment, including regular
2 doses. 31–44 KG: 4 mg once wkly for monitoring of blood counts. • Report
2 doses. 21–30 KG: 2.5 mg once wkly unusual fever or chills, severe bone pain,
for 2 doses. 10–20 KG: 1.5 mg once wkly chest pain or palpitations.
for 2 doses. LESS THAN 10 KG: 0.1 mg/kg
once wkly for 2 doses.
pegloticase
Dosage in Renal/Hepatic Impairment
No dose adjustment. peg-loe-ti-kase
(Krystexxa)
SIDE EFFECTS j BLACK BOX ALERT j Severe
Frequent (72%–15%): Bone pain, nausea, infusion reactions, anaphylaxis
fatigue, alopecia, diarrhea, vomiting, (bronchospasm, stridor, urticaria,
constipation, anorexia, abdominal pain, hypotension, dyspnea, flushing, cir-
cumoral swelling) have occurred,
arthralgia, generalized weakness, periph- especially within 2 hrs of first infu-
eral edema, dizziness, stomatitis, mucosi- sion. Premedicate pt with corticos-
tis, neutropenic fever. teroids, antihistamines. Should be
administered in health care setting
ADVERSE EFFECTS/TOXIC by health care providers prepared
REACTIONS to manage infusion reactions. Life-
threatening hemolytic reaction and
Allergic reactions (anaphylaxis, rash, ur- methemoglobinemia reported in pts
ticaria) occur rarely. Cytopenia resulting with G6PD deficiency.

underlined – top prescribed drug


pegloticase 919
Do not confuse pegloticase with AVAILABILITY (Rx)
Activase, cholinesterase, or Injection Solution: 2-mL (8 mg/mL)
pegaspargase. single-use vials.
uCLASSIFICATION ADMINISTRATION/HANDLING
PHARMACOTHERAPEUTIC: Uric acid
IV
enzyme. CLINICAL: Antigout agent.
Reconstitution • Withdraw 1 mL
from single-use vial and inject into 250
USES mL 0.9% NaCl or 0.45% NaCl. • Invert
Treatment of chronic gout in adult pts infusion bag a number of times to ensure
refractory to conventional therapy. Not thorough mixing; do not shake.
recommended for treatment of asymp- Rate of administration • Infuse slowly
tomatic hyperuricemia. over no less than 120 min.
Storage • Store in refrigerator. • So-
PRECAUTIONS lution should appear clear; discard if
Contraindications: Hypersensitivity to particulate is present. • Allow diluted
pegloticase. Glucose-6-phosphate de- solution to reach room temperature prior
hydrogenase (G6PD) deficiency due to infusion. • Following dilution, solu-
to hemodialysis, methemoglobinemia. tion remains stable for 4 hrs if refriger-
­ autions: History of HF, elderly, debili-
C ated or at room temperature.
tated.
INDICATIONS/ROUTES/DOSAGE
ACTION b ALERT c   Give by IV infusion; do not give
Decreases uric acid production by cata- as IV push or IV bolus. Pt to be pretreated
lyzing oxidation of uric acid to allantoin, with corticosteroids, antihistamines to re-
lowering serum uric acid. Therapeutic duce risk of infusion reaction, anaphylaxis.
Effect: Lowers serum uric acid concen- P
tration. Gout
Note: Discontinue oral agents prior to
PHARMACOKINETICS initiating pegloticase and do not initiate
Catalyzes oxidation of uric acid to allan- during course of therapy.
toin, an inert and water-soluble purine IV infusion: ADULTS, ELDERLY: 8 mg
metabolite. Readily eliminated, primarily every 2 wks.
by renal excretion. Half-life: 14.5 days.
Dosage in Renal/Hepatic Impairment
LIFESPAN CONSIDERATIONS No dose adjustment.
Pregnancy/Lactation: Unknown if SIDE EFFECTS
drug crosses placenta or is distributed
in breast milk. Children: Safety and ef- Occasional (12%–9%): Nausea, ecchy-
ficacy not established. Elderly: No age- mosis at IV site, nasopharyngitis. Rare
(6%–5%): Constipation, vomiting.
related precautions noted.
INTERACTIONS ADVERSE EFFECTS/TOXIC
REACTIONS
DRUG: May decrease effect of pegfilgras-
tim. Allopurinol, febuxostat, pro- Exacerbation of HF has been noted. Infu-
benecid may increase adverse effects. sion-related reaction (urticaria, dyspnea,
HERBAL: None significant. FOOD: None
chest discomfort, chest pain, erythema,
known. LAB VALUES: Decreases serum pruritus) occurs in 26% of pts; anaphy-
uric acid (expected). laxis occurs in 7% of pts. Increase in gout
flares is frequently noted upon initiation

Canadian trade name Non-Crushable Drug High Alert drug


920 pembrolizumab
of antihyperuricemic therapy due to USES
changing serum uric acid levels. Treatment of unresectable or metastatic
melanoma. Treatment of metastatic head
NURSING CONSIDERATIONS
and neck squamous cell carcinoma (HN-
BASELINE ASSESSMENT SCC) (recurrent or metastatic) with disease
If gout flare occurs during treatment, pro- progression on or after platinum-contain-
phylaxis with an NSAID or colchicine is ing chemotherapy. Treatment of metastatic
recommended. Pts at higher risk for G6PD non–small-cell lung cancer (NSCLC) in pts
deficiency (e.g., pts of African or Mediter- with PD-L1–expressing tumors as a single
ranean ancestry) should be screened for agent for first-line tx, with disease pro-
G6PD deficiency before starting therapy. gression on or after platinum-containing
Obtain serum uric acid levels prior to chemotherapy; or in combination with
each infusion. If levels reach greater than pemetrexed and carboplatin, as first-line
6 mg/dL, particularly when 2 consecutive tx of metastatic non-squamous NSCLC
levels greater than 6 mg/dL are observed, or as first-line single-agent treatment of
treatment should be discontinued. metastatic NSCLC in pts with tumors with
PD-L1 expression and with no EGFR or ALK
INTERVENTION/EVALUATION genomic tumor aberrations. Treatment of
Monitor closely for infusion reaction dur- refractory classical Hodgkin lymphoma
ing therapy and for 2 hrs post-treatment. (cHL) or relapse after 3 or more lines of
If infusion reaction occurs during ad- therapy. Treatment of locally advanced or
ministration, infusion may be slowed, or metastatic urothelial carcinoma not eligi-
stopped and restarted at slower rate. If ble for cisplatin-containing chemotherapy
severe infusion reaction occurs, discon- or who have disease progression during
tinue infusion and institute treatment as or following platinum-containing chemo-
needed. Assess for therapeutic response therapy; or with 12 mos of neoadjuvant
(reduced joint tenderness, swelling, red- or adjuvant tx with platinum-containing
P ness, limitation of motion). chemotherapy. Treatment of unresectable
or metastatic microsatellite instability high
PATIENT/FAMILY TEACHING
(MSI-H) or mismatch repair deficient solid
• Educate pts on the most common signs tumors or colorectal cancer. Treatment of
and symptoms of infusion reaction (rash, gastric cancer (advanced or metastatic)
redness of skin, difficulty breathing, flush- or gastroesophageal junction adenocar-
ing, chest discomfort, chest pain). • Ad- cinoma in pts with tumors with PD-L1
vise pts to seek medical care immediately if expression and with disease progression
they experience any symptoms of allergic on or after 2 or more lines of therapy.
reaction during or at any time after infusion. Treatment of recurrent or metastatic cervi-
cal cancer in pts with tumors with PD-L1
expression and with disease progression
pembrolizumab on or after chemotherapy. Treatment of
primary mediastinal large B-cell lym-
pem-broe-liz-ue-mab phoma (PMBCL) in adult and pediatric
(Keytruda) pts with refractory disease or relapsed
Do not confuse pembrolizumab after 2 or more lines of therapy. Treat-
with palivizumab. ment of hepatocellular carcinoma in pts
previously treated with sorafenib. Adjuvant
uCLASSIFICATION treatment of melanoma with lymph node
PHARMACOTHERAPEUTIC: Anti involvement following complete resection.
PD-1 monoclonal antibody. CLINI- Treatment of recurrent locally advanced or
CAL: Antineoplastic. metastatic Merkel cell carcinoma. Treat-
ment of advanced renal cell carcinoma (in
underlined – top prescribed drug
pembrolizumab 921
combination with axitinib). Treatment of ­VALUES: May increase serum AST, glu-
metastatic small-cell lung cancer (SCLC) cose, triglycerides. May decrease albu-
in pts with disease progression on or after min, serum calcium, sodium.
platinum-based chemotherapy and at least
one other prior line of therapy. Treatment AVAILABILITY (Rx)
of HNSCC. Treatment of metastatic squa- Injection Solution: 100 mg/4 mL.
mous cell carcinoma of esophagus. Treat- ADMINISTRATION/HANDLING
ment of advanced endometrial carcinoma
(in combination with lenvatinib) that is not IV
MSI-H or dMMR, having disease progres- b ALERT c Use 0.2–0.5-micron in-line
sion following prior systemic therapy, and filter.
who are not candidates for curative surgery Reconstitution • Withdraw required
or radiation. dose and mix into 0.9% NaCl infusion
PRECAUTIONS bag (diluent volume depends on dose
required). • Final concentration of di-
Contraindications: Hypersensitivity to luent bag should equal 1–10 mg/
pembrolizumab. Cautions: Thyroid dis- mL. • Allow refrigerated solution to
ease, hepatic/renal impairment, intersti- warm to room temperature before
tial lung disease, electrolyte imbalance, ­infusing.
hypertriglyceridemia. Rate of administration • Infuse via
ACTION dedicated line over 30 min using a
0.2–0.5-micron filter.
Binds PD-1 ligands to PD-1 receptor Storage • Diluted solution up to 24
found on T cells, blocking its interaction hrs, or at room temperature up to 4 hrs.
with the ligands (PD-L1 and PD-L2). Re- Store time should not exceed total com-
leases PD-1 pathway–mediated inhibition bined time of reconstitution, dilution,
of immune response (including antitu- storage, and infusion.
mor immune response). Therapeutic P
Effect: Inhibits T-cell proliferation and INDICATIONS/ROUTES/DOSAGE
cytokine production. Induces antitumor cHL, MSI-H Cancer
responses. IV: ADULTS, ELDERLY: 200 mg q3wks
PHARMACOKINETICS until disease progression or unaccept-
able toxicity. CHILDREN: 2 mg/kg (up to
Metabolism not specified. Elimination 200 mg) q3wks until disease progression
not specified. Steady-state concentration: or unacceptable toxicity.
18 wks. Half-life: 26 days.
Cervical Cancer, Gastric Cancer, HNSCC,
LIFESPAN CONSIDERATIONS NSCLC (Single-Agent Therapy), Primary
Pregnancy/Lactation: Avoid pregnancy; Mediastinal Large B-Cell Lymphoma,
may cause fetal harm. Unknown if distrib- Melanoma, Urothelial Cancer,
uted in breast milk. Females of reproduc- Hepatocellular Carcinoma, Head
tive potential must use effective contracep- and Neck Squamous Cell, Melanoma
tion during treatment and up to 4 mos after (Adjuvant Treatment), Merkel Cell
discontinuation. Children: Safety and Carcinoma, Renal Cell Carcinoma, SCLC,
efficacy not established. Elderly: No age- Squamous Cell Carcinoma of Esophagus,
related precautions noted. Endometrial Carcinoma
IV: ADULTS, ELDERLY: 200 mg q3wks.
INTERACTIONS Continue until disease progression or
DRUG: None known. HERBAL: None unacceptable toxicity, or in pts without
significant. FOOD: None known. LAB disease progression.

Canadian trade name Non-Crushable Drug High Alert drug


922 pembrolizumab
NSCLC (Combination Therapy) Occasional (18%–11%): Dyspnea, ex-
IV: ADULTS, ELDERLY: 200 mg q3wks tremity pain, peripheral edema, vomit-
(in combination with pemetrexed and ing, headache, chills, insomnia, myalgia,
carboplatin) for 4 cycles, then 200 mg abdominal pain, back pain, pyrexia, vit-
q3wks (with or without optional indefi- iligo, dizziness, upper respiratory tract
nite pemetrexed maintenance therapy). infection.
Continue until disease progression or
unacceptable toxicity, or in pts with- ADVERSE EFFECTS/TOXIC
out disease progression for up to 24 REACTIONS
months. May cause severe immune-mediated
events such as pneumonitis (2.9% of
Dose Modification pts), colitis (1% of pts), hepatitis (0.5%
Based on Common Terminology Criteria of pts), hypophysitis (0.5% of pts), renal
for Adverse Events (CTCAE). failure or nephritis (0.7% of pts), hyper-
Withhold treatment for any of the thyroidism (1.2% of pts), hypothyroid-
following adverse events: ALT or ism (8.3% of pts). Other reported events
AST greater than 3–5 times upper limit include adrenal insufficiency, arthritis,
of normal (ULN) or bilirubin 1.5–3 times cellulitis, exfoliative dermatitis, hemolytic
ULN, Grade 2 or 3 colitis, Grade 3 hyper- anemia, myositis, myasthenic syndrome,
thyroidism, Grade 2 nephritis, Grade 2 pancreatitis, partial seizures, pneumonia,
pneumonitis, symptomatic hypophysitis; optic neuritis, rhabdomyolysis, sepsis.
any Grade 3 treatment-related adverse Immunogenicity (anti-pembrolizumab
reaction. Permanently discontinue antibody formation) may occur.
for any of the following adverse
events: ALT or AST greater than 5 times NURSING CONSIDERATIONS
ULN or bilirubin 3 times ULN (or pts with
BASELINE ASSESSMENT
liver metastasis who begin treatment with
Grade 2 ALT, AST, if ALT or AST increases Obtain baseline CBC, BMP, ionized
P
greater than or equal to 50% from base- calcium, LFT, TSH, free T4, vital signs,
line and lasts for at least 1 wk), Grade 3 urine pregnancy. Obtain weight in kg.
or 4 infusion-related reaction, Grade 3 or Screen for history of adrenal/pituitary/
4 nephritis, Grade 3 or 4 pneumonitis; in- pulmonary/thyroid disease, autoimmune
ability to reduce corticosteroid dose to 10 disorders, hepatic/renal impairment, al-
mg/day or less (or predniSONE equiva- lergy to predniSONE. Question plans for
lent) after last dose; persistent Grade 2 or breastfeeding. Along with routine assess-
3 adverse reaction that does not recover ment, conduct full dermatologic exam,
to Grade 0–1 within 12 wks after last visual acuity.
dose; any severe or Grade 3 treatment- INTERVENTION/EVALUATION
related adverse reaction that reoccurs.
Monitor CBC, LFT, serum electrolytes;
Dosage in Renal Impairment thyroid panel if applicable. Monitor for
No dose adjustment. immune-mediated adverse events. Notify
physician if any CTCAE toxicities occur
Dosage in Hepatic Impairment (see Appendix M) and initiate proper
Mild impairment: No dose adjustment. treatment. Obtain chest X-ray if pneu-
Moderate to severe impairment: Not monitis suspected. Screen for tumor
studied, use caution. lysis syndrome in pts with high tumor
burden. Offer antiemetics if nausea, vom-
SIDE EFFECTS iting occurs. Monitor I&O, daily weight.
Frequent (47%–20%): Fatigue, nausea, If predniSONE therapy initiated, monitor
cough, pruritus, rash, decreased appe- capillary blood glucose and screen for
tite, constipation, diarrhea, arthralgia. corticosteroid side effects.
underlined – top prescribed drug
PEMEtrexed 923
PATIENT/FAMILY TEACHING PRECAUTIONS
• Blood levels will be routinely moni- Contraindications: Severe hypersensitivity
tored. • Avoid pregnancy; treatment may to PEMEtrexed. Cautions: Hepatic/renal
cause birth defects or miscarriage. Do not impairment, concurrent use of nephrotoxic
breastfeed. • Serious adverse reactions medications, preexisting myelosuppression.
may affect lungs, GI tract, kidneys, or Not indicated for squamous cell NSCLC.
hormonal glands, and predniSONE ther-
apy may need to be started. • Immedi- ACTION
ately contact physician if serious or life- Inhibits biosynthesis of purine and thy-
threatening inflammatory reactions occur midine nucleotides. Inhibits protein syn-
in the following body systems: lung (chest thesis. Therapeutic Effect: Disrupts
pain, cough, shortness of breath); colon folate-dependent enzymes essential for
(severe abdominal pain or diarrhea); cell replication.
liver (bruising, clay-colored/tarry stools,
yellowing of skin or eyes); pituitary (per- PHARMACOKINETICS
sistent or unusual headache, dizziness, Protein binding: 81%. Not metabolized.
extreme weakness, fainting, vision Excreted in urine. Half-life: 3.5 hrs.
changes); kidney (decreased or dark-
colored urine, flank pain); thyroid (in- LIFESPAN CONSIDERATIONS
somnia, hypertension, tachycardia [over- Pregnancy/Lactation: Avoid pregnancy;
active thyroid]), (fatigue, goiter, weight may cause fetal harm. Females of repro-
gain [underactive thyroid]). ductive potential must use effective contra-
ception during treatment and for at least
6 mos after discontinuation. Unknown if
distributed in breast milk. Breastfeeding
PEMEtrexed not recommended during treatment and
for at least 7 days after discontinuation.
pem-e-trex-ed Males must use effective contraception dur- P
(Alimta) ing treatment and for at least 3 mos after
discontinuation. Children: Safety and effi-
uCLASSIFICATION cacy not established in pts younger than 18
PHARMACOTHERAPEUTIC: Folate yrs. Elderly: Higher incidence of fatigue,
analog metabolic inhibitor. Antime- leukopenia, neutropenia, thrombocytope-
tabolite. CLINICAL: Antineoplastic. nia in pts 65 yrs and older.
Do not confuse PEMEtrexed with
methotrexate or PRALAtrexate. INTERACTIONS
DRUG: Ibuprofen may increase con-
centration/adverse effects. Bone mar-
USES row depressants (e.g., cladribine)
Treatment of unresectable malignant may increase risk of myelosuppression.
pleural mesothelioma in combination Live virus vaccines may potentiate vi-
with CISplatin. Initial treatment of locally rus replication, increase vaccine side
advanced or metastatic nonsquamous effects, decrease pt’s antibody response
non–small-cell lung cancer (NSCLC) in to vaccine. HERBAL: Echinacea may de-
combination with CISplatin. Single-agent crease effects. FOOD: None known. LAB
maintenance treatment of NSCLC in pts VALUES: May increase serum ALT, AST,
whose disease has not progressed follow- creatinine.
ing 4 cycles of platinum-based first-line
chemotherapy. OFF-LABEL: Treatment of AVAILABILITY (Rx)
bladder, cervical, ovarian, thymic malig- Injection, Powder for Reconstitution: 100
nancies; malignant pleural mesothelioma. mg; 500 mg.

Canadian trade name Non-Crushable Drug High Alert drug


924 PEMEtrexed

ADMINISTRATION/HANDLING agent). Continue until disease progres-


sion or unacceptable toxicity.
IV Infusion
Reconstitution • Dilute 500-mg vial Dose Modification for Hematologic
with 20 mL (4.2 mL to 100-mg vial) 0.9% Toxicity
NaCl to provide concentration of 25 mg/ Nadir ANC less than 500 cells/mm3
mL. • Gently swirl each vial until powder and platelets 50,000 cells/mm3 or
is completely dissolved. • Solution ap- more: Reduce dose to 75% of previous
pears clear and ranges in color from color- dose. Nadir platelets less than 50,000
less to yellow or green-yellow. • Further cells/mm3 without bleeding: Reduce
dilute reconstituted solution with 100 mL dose to 75% of previous dose. Nadir plate-
0.9% NaCl. lets less than 50,000 cells/mm3 with
Rate of administration • Infuse over bleeding: Reduce dose to 50% of previous
10 min. dose. Nonhematologic toxicity Grade
Storage • Store at room temperature. 3 or greater (excluding neurotoxic-
• Diluted solution is stable for up to 24 ity): Reduce dose to 75% of previous dose
hrs at room temperature or if refrigerated. (excluding mucositis). Grade 3 or 4 muco-
sitis: Reduce dose to 50% of previous dose.
IV INCOMPATIBILITIES
Dosage in Renal Impairment
Use only 0.9% NaCl to reconstitute; flush
line prior to and following infusion. Do Not recommended with CrCl less than
not add any other medications to IV line. 45 mL/min.
Dosage in Hepatic Impairment
INDICATIONS/ROUTES/DOSAGE
Grade 3 (5.1–20 times ULN) or Grade
b ALERT c Pretreatment with dexametha- 4 (greater than 20 times ULN): 75%
sone (or equivalent) will reduce risk, se- of previous dose.
verity of cutaneous reaction; treatment with
P folic acid and vitamin B12 beginning 1 wk SIDE EFFECTS
before treatment and continuing for 21 Frequent (12%–10%): Fatigue, nausea,
days after last PEMEtrexed dose will reduce vomiting, rash, desquamation. Occa-
risk of side effects. Do not begin new treat- sional (8%–4%): Stomatitis, pharyngitis,
ment cycles unless ANC 1,500 cells/mm3 or diarrhea, anorexia, hypertension, chest
greater, platelets 100,000 cells/mm3 or pain. Rare (less than 3%): Constipation,
greater, and CrCl 45 mL/min or greater. depression, dysphagia.
Malignant Pleural Mesothelioma ADVERSE EFFECTS/TOXIC
IV: ADULTS, ELDERLY: 500 mg/m2 on day REACTIONS
1 of each 21-day cycle in combination
Myelosuppression, characterized as CT-
with CISplatin. Continue until disease
CAE Grade 1–4 neutropenia, thrombo-
progression or unacceptable toxicity.
cytopenia, anemia, was reported. Severe,
Nonsquamous Non–Small-Cell Lung sometimes fatal renal toxicity may oc-
Cancer (NSCLC) cur. Serious cutaneous events including
IV: ADULTS, ELDERLY: Initial treatment bullous, blistering, and exfoliative skin
500 mg/m2 on day 1 of each 21-day cycle toxicities, Stevens-Johnson syndrome,
(in combination with CISplatin) for up to epidermal necrolysis may occur. Fatal
6 cycles or until disease progression or cases of interstitial pneumonitis were
unacceptable toxicity. Maintenance or reported. Radiation recall may occur in
second-line treatment: 500 mg/m2 pts who have received radiation wks to
on day 1 of each 21-day cycle (as single yrs previously.

underlined – top prescribed drug


penicillin G p­ otassium 925

NURSING CONSIDERATIONS penicillin G


BASELINE ASSESSMENT
Obtain CBC, BMP, LFT; pregnancy test in
­potassium
females of reproductive potential. Ques- pen-i-sil-in G po-tas-ee-um
tion current breastfeeding status. Verify (Crystapen , Pfizerpen-G)
use of contraception in female pts of re- Do not confuse penicillin with
productive potential. Question history of penicillAMINE.
hepatic/renal impairment. Receive full
medication history and screen for inter- uCLASSIFICATION
actions (esp. use of NSAIDs). Assess hy- PHARMACOTHERAPEUTIC: Penicil-
dration status. Offer emotional support. lin. CLINICAL: Antibiotic.
INTERVENTION/EVALUATION
Monitor CBC as clinically indicated; BMP, USES
LFT periodically. Monitor for hemato-
Treatment of susceptible infections in-
logic toxicity (fever, sore throat, signs of
cluding sepsis, meningitis, endocarditis,
local infection, unusual bruising/bleed-
pneumonia. Active against gram-positive
ing from any site), symptoms of anemia
organisms (except S. aureus), some
(excessive fatigue, weakness), renal tox-
gram-negative organisms (e.g., N. gon-
icity. Assess skin for rash, lesions, derma-
orrhoeae), and some anaerobes and
tological toxicities. Obtain CXR if intersti-
spirochetes.
tial lung disease, pneumonitis suspected.
Ensure adequate hydration. PRECAUTIONS
PATIENT/FAMILY TEACHING Contraindications: Hypersensitivity to
• Treatment may depress your immune any penicillin. Cautions: Renal/hepatic
system response and reduce your ability to impairment, seizure disorder, hyper-
sensitivity to cephalosporins, pts with P
fight infection. Report symptoms of infec-
tion such as body aches, chills, cough, asthma.
­fatigue, fever. Avoid those with active infec-
ACTION
tion. • Use effective contraception dur-
ing treatment and for at least 6 mos after Inhibits bacterial cell wall synthesis by
last dose. Do not breastfeed during treat- binding to one or more of the penicillin-
ment and for at least 7 days after last dose. binding proteins of bacteria. Therapeu-
Males must use barrier methods (e.g., tic Effect: Bactericidal.
condoms) with sexual activity during
PHARMACOKINETICS
treatment and for at least 3 mos after last
dose. • Report unusual bruising or Protein binding: 60%. Widely distributed
bleeding of any kind. • Treatment may (poor CNS penetration). Metabolized in
cause severe lung inflammation; report liver. Primarily excreted in urine. Half-
cough, difficulty breathing, fever. • Re- life: 0.5–1 hr (increased in renal im-
port skin toxicities such as blistering, bub- pairment).
bling, sloughing of the skin; liver prob-
LIFESPAN CONSIDERATIONS
lems (bruising, confusion, amber- or
orange-colored urine, abdominal pain, Pregnancy/Lactation: Readily crosses
yellowing of the skin or eyes); kidney placenta; distributed in breast milk.
problems (decreased urine output, dark- Children: May delay renal excretion in
colored urine, flank pain). • Pts with neonates, young infants. Elderly: Age-
history of renal impairment should avoid related renal impairment may require
NSAIDs (e.g., ibuprofen). dosage adjustment.

Canadian trade name Non-Crushable Drug High Alert drug


926 penicillin G ­potassium

INTERACTIONS Creatinine
Clearance Dosage
DRUG: Probenecid increases con-
centration. HERBAL: None significant. Greater than 50 mL/ No dose adjustment
FOOD: None significant. LAB VAL- min
10–50 mL/min 75% normal dose
UES: May cause positive Coombs’ test. Less than 10 mL/ 20%–50% normal
May increase serum ALT, AST, alkaline min dose
phosphatase, LDH. May decrease WBC Hemodialysis 50%–100% normal
count. dose q8–12h
Continuous renal
AVAILABILITY (Rx) replacement
Injection, Powder for Reconstitution: 5 t­herapy
Continuous Loading dose 4 mil-
million units.
venovenous lion units, then 2
hemofiltration million units q4–6h
ADMINISTRATION/HANDLING Continuous Loading dose 4 mil-
IV venovenous lion units, then 2–3
hemodialysis million units q4–6h
Reconstitution • After reconstitution, Continuous Loading dose 4 mil-
further dilute with 50–100 mL D5W or venovenous lion units, then 2–4
0.9% NaCl for final concentration of hemodiafiltration million units q4–6h
100,000–500,000 units/mL (50,000
units/mL for infants, neonates). Dosage in Hepatic Impairment
Rate of administration • Infuse over No dose adjustment.
15–30 min.
Storage • Reconstituted solution is SIDE EFFECTS
stable for 7 days if refrigerated. Occasional: Lethargy, fever, dizziness,
rash, electrolyte imbalance, diarrhea,
IV INCOMPATIBILITIES thrombophlebitis. Rare: Seizures, inter-
P DOPamine (Intropin), sodium bicar- stitial nephritis.
bonate.
ADVERSE EFFECTS/TOXIC
IV COMPATIBILITIES REACTIONS
Amiodarone (Cordarone), calcium Hypersensitivity reactions ranging from
gluconate, dilTIAZem (Cardizem), rash, fever, chills to anaphylaxis occur
heparin, magnesium sulfate, potassium occasionally.
chloride.
NURSING CONSIDERATIONS
INDICATIONS/ROUTES/DOSAGE
BASELINE ASSESSMENT
Usual Dosage
IV, IM: ADULTS, ELDERLY: 12–24 million Question for history of allergies, particu-
units/day in divided doses q4–6h. CHILDREN: larly penicillins, cephalosporins.
Mild to moderate infection: 100,000– INTERVENTION/EVALUATION
150,000 units/kg/day in divided doses q6h. Promptly report rash (hypersensitivity),
Maximum: 8 million units/day. Severe in- diarrhea (with fever, abdominal pain,
fections: 200,000–300,000 units/kg/day mucus, or blood in stool, may indicate
in divided doses q4–6h. Maximum: 24 antibiotic-associated colitis). Monitor
million units/day. NEONATES: 25,000– I&O, urinalysis electrolytes, renal func-
50,000 units/kg/dose q8–12h. tion tests for nephrotoxicity.
Dosage in Renal Impairment
Dosage interval is modified based on cre-
atinine clearance.

underlined – top prescribed drug


penicillin V p­ otassium 927

INTERACTIONS
penicillin V DRUG: May increase concentration/
­potassium effect of methotrexate. Probenecid
may increase concentration, risk of
pen-i-sil-in V po-tas-ee-um toxicity. Tetracycline may decrease
(Apo-Pen-VK , Novo-Pen-VK , concentration/effect. HERBAL: None
NuPen VK ) significant. FOOD: None known. LAB
VALUES: May cause positive Coombs’
uCLASSIFICATION test. May increase serum ALT, AST, al-
PHARMACOTHERAPEUTIC: Penicil- kaline phosphatase, LDH. May decrease
lin. CLINICAL: Antibiotic. WBC count.
AVAILABILITY (Rx)
USES Powder for Oral Solution: 125 mg/5 mL,
Treatment of infections of respiratory tract, 250 mg/5 mL. Tablets: 250 mg, 500 mg.
skin/skin structure, otitis media, necrotiz-
ing ulcerative gingivitis; prophylaxis for ADMINISTRATION/HANDLING
rheumatic fever, dental procedures. OFF- PO
LABEL: Prosthetic joint infection. • Give on empty stomach 1 hr before or 2
hrs after meals (increases absorp-
PRECAUTIONS tion). • After reconstitution, oral solution
Contraindications: Hypersensitivity to is stable for 14 days if refrigerated. • Space
any penicillin. Cautions: Severe renal doses evenly around the clock.
impairment, history of allergies (particu-
larly cephalosporins), history of seizures, INDICATIONS/ROUTES/DOSAGE
asthma. Usual Dosage
PO: ADULTS, ELDERLY, CHILDREN 12 YRS
ACTION AND OLDER: 125–500 mg q6–8h. CHIL- P
Inhibits cell wall synthesis by binding to DREN YOUNGER THAN 12 YRS: 25–75 mg/
bacterial cell membranes. Therapeutic kg/day in divided doses q6–8h. Maxi-
Effect: Bactericidal. mum: 2,000 mg/day.
PHARMACOKINETICS Dosage in Renal/Hepatic Impairment
Moderately absorbed from GI tract. Pro- No dose adjustment.
tein binding: 80%. Widely distributed. SIDE EFFECTS
Metabolized in liver. Primarily excreted
in urine. Half-life: 1 hr (increased in Frequent: Mild hypersensitivity reaction
renal impairment). (chills, fever, rash), nausea, vomiting,
diarrhea. Rare: Bleeding, allergic reac-
LIFESPAN CONSIDERATIONS tion.
Pregnancy/Lactation: Readily crosses ADVERSE EFFECTS/TOXIC
placenta; appears in cord blood, amni- REACTIONS
otic fluid. Distributed in breast milk in
low concentrations. May lead to allergic Severe hypersensitivity reactions, in-
sensitization, diarrhea, candidiasis, skin cluding anaphylaxis, may occur. Neph-
rash in infant. Children: Use caution in rotoxicity, antibiotic-associated colitis,
neonates and young infants (may delay other superinfections (abdominal
renal elimination). Elderly: Age-related cramps, severe watery diarrhea, fever)
renal impairment may require dosage may result from high dosages, pro-
adjustment. longed therapy.

Canadian trade name Non-Crushable Drug High Alert drug


928 perampanel

NURSING CONSIDERATIONS adjunct or monotherapy in pts 4 yrs of age


and older. Adjunctive therapy for the treat-
BASELINE ASSESSMENT ment of primary generalized tonic-clonic
Question for history of allergies, particu- seizures in pts 12 yrs and older.
larly penicillins, cephalosporins.
PRECAUTIONS
INTERVENTION/EVALUATION Contraindications: Hypersensitivity to per­
Hold medication, promptly report rash ampanel. Cautions: Elderly (increased
(hypersensitivity), diarrhea (with fever, falls, dizziness, gait disturbances), severe
abdominal pain, mucus or blood in stool renal/hepatic impairment, dialysis, con-
may indicate antibiotic-associated colitis). current use of CNS depressants, pts at
Be alert for superinfection: fever, vomiting, risk for suicidal behavior.
diarrhea, anal/genital pruritus, oral muco-
sal change (ulceration, pain, erythema). ACTION
Review Hgb levels; check for bleeding Noncompetitive antagonist of AMPA glu-
(overt/occult bleeding, ecchymosis, swell- tamate receptors, a primary excitatory
ing of tissue). Monitor I&O, urinalysis, re- neurotransmitter on postsynaptic neu-
nal function tests for nephrotoxicity. rons. Therapeutic Effect: Reduces
PATIENT/FAMILY TEACHING
frequency of seizure activity.
• Continue antibiotic for full length of PHARMACOKINETICS
treatment. • Space doses evenly. • Re-
port immediately if rash, diarrhea, bleed- Rapidly, completely absorbed. Peak con-
ing, bruising, other new symptoms occur. centration: 0.5–2.5 hrs. Protein binding:
95%–96%. Steady state reached in 2–3
wks. Metabolized via oxidation/glucuron-
idation. Excreted in feces (48%), urine
perampanel (22%). Half-life: 105 hrs.
P
per-am-pa-nel LIFESPAN CONSIDERATIONS
(Fycompa)
Pregnancy/Lactation: Unknown if
j BLACK BOX ALERT j Risk for distributed in breast milk. Use caution
serious neuropsychiatric events, in-
cluding irritability, aggression, anger, when breastfeeding. Children: Safety
anxiety, paranoia, euphoric mood, ag- and efficacy not established in pts
itation, mental status changes. Some younger than 12 yrs. Elderly: Due to
of these events reported as serious increased risk of adverse reactions in the
and life-threatening. Violent thoughts
or threatening behavior were also elderly, dosing titration should proceed
observed. Immediately report any very slowly.
changes in mood or behavior that are
not typical for the patient. Health care INTERACTIONS
professionals should closely monitor DRUG: CYP450 inducers (e.g., car-
patients during titration period when
higher doses are used. BAMazepine, OXcarbazepine, phe-
nytoin) may decrease concentration/
uCLASSIFICATION effects. May decrease effectiveness of
PHARMACOTHERAPEUTIC: AMPA hormonal contraceptives contain-
glutamate receptive antagonist. CLIN- ing levonorgestrel. Alcohol, other
ICAL: Anticonvulsant. CNS depressants (e.g., LORazepam,
morphine, zolpidem) may increase
CNS depression. HERBAL: St. John’s
USES wort may decrease concentration/­
Treatment of partial-onset seizures with or effect. Herbals with sedative prop-
without secondary generalized seizures as erties (e.g., chamomile, kava kava,
underlined – top prescribed drug
perampanel 929
valerian) may increase CNS depres- increments at wkly intervals (in elderly,
sion. FOOD: None known. LAB VALUES: no more frequently than q2wks). Rec-
None significant. ommended maintenance dose: 8–12
mg/day at bedtime.
AVAILABILITY (Rx)
Dosage in Renal Impairment
Suspension, Oral: 0.5 mg/mL. Tab-
lets, Film-Coated: 2 mg, 4 mg, 6 mg, 8 CrCl less than 30 mL/min: Not rec-
mg, 10 mg, 12 mg. ommended.
Dosage in Hepatic Impairment
ADMINISTRATION/HANDLING
PO: ADULTS, ELDERLY, CHILDREN 12 YRS
PO AND OLDER: 2 mg once daily with wkly
• Give at bedtime. • Give tablet whole; increase of 2 mg daily q2wks until tar-
do not break, crush, dissolve, or divide get dose is achieved. Mild impairment:
tablet. • Measure oral suspension us- Maximum: 6 mg. Moderate impair-
ing provided adapter and dosing syringe. ment: Maximum: 4 mg. Severe im-
INDICATIONS/ROUTES/DOSAGE pairment: Not recommended.
b ALERT c Initial starting dose should SIDE EFFECTS
be increased when enzyme-inducing anti- Frequent (32%–11%): Dizziness, sleepi-
convulsants are given concurrently. Indi- ness, headache. Occasional (8%–
vidual dosing based on clinical response, 3%): Fatigue, irritability, nausea, balance
tolerability. Do not use in severe hepatic/ disorder, weight gain, gait disturbance,
renal impairment, pts on hemodialysis. vertigo, blurred vision, vomiting, arthral-
gia, anxiety. Rare (2%–1%): Constipation,
Partial-Onset Seizures in Absence of an back pain, extremity pain, asthenia, oro-
Enzyme-Inducing Anticonvulsant pharyngeal pain, aggression.
PO: ADULTS, ELDERLY, CHILDREN 4 YRS AND
OLDER: Initially, 2 mg once daily at bed- ADVERSE EFFECTS/TOXIC P
time. May titrate in 2-mg increments at wkly REACTIONS
intervals (in elderly, no more frequently Irritability, aggression, anger, anxiety, af-
than every 2 wks). Recommended main- fect lability, agitation occurred rarely (2%
tenance dose: 8–12 mg/day at bedtime. of pts). Increased risk for seizures when
Generalized Tonic-Clonic Seizures
anticonvulsants are withdrawn abruptly.
in Absence of an Enzyme-Inducing NURSING CONSIDERATIONS
Anticonvulsant
PO: ADULTS, ELDERLY, CHILDREN 12 YRS BASELINE ASSESSMENT
AND OLDER: Initially, 2 mg once daily at Review history of seizure disorder (in-
bedtime. May titrate in 2-mg increments tensity, frequency, duration, LOC). Initiate
at wkly intervals (in elderly, no more seizure precautions. Obtain medication his-
frequently than every 2 wks). Recom- tory (esp. use of other anticonvulsant ther-
mended maintenance dose: 8-12 mg/ apy; dosage based on concurrent seizure
day at bedtime. medication). Observe clinically. Assist with
ambulation until response to drug is estab-
Partial-Onset Seizures, Generalized Tonic- lished (32% of pts experience dizziness).
Clonic Seizures (Concurrently Taking an
Enzyme-Inducing Anticonvulsant) INTERVENTION/EVALUATION
PO: ADULTS, ELDERLY, CHILDREN 12 YRS Assess mental status, cognitive abilities,
AND OLDER (4 YRS AND OLDER FOR PARTIAL- behavioral changes. Monitor for clinical
ONSET SEIZURES): Initially, 4 mg once response, tolerability to medication, dosing
daily at bedtime. May titrate in 2-mg level during treatment and for at least 1 mo

Canadian trade name Non-Crushable Drug High Alert drug


930 pertuzumab
after last therapy dose. Report persistent, PRECAUTIONS
severe, or worsening psychiatric symptoms Contraindications: Hypersensitivity to
or behaviors. Assess for clinical improve- pertuzumab. Cautions: Conditions that
ment (decrease in intensity, frequency of may impair left ventricular function
seizures). (e.g., uncontrolled hypertension, recent
PATIENT/FAMILY TEACHING MI, severe cardiac arrhythmia), his-
tory of infusion-related reaction. Prior
• Avoid alcohol (greater risk for ad-
anthracycline therapy or irradiation.
verse effects). • The combination of
Conditions predisposing to infection
alcohol and perampanel may signifi-
(e.g., diabetes, immunocompromised
cantly worsen mood, increase an-
pts, renal failure, open wounds), pts
ger. • Counsel pts, families, and care-
at risk for tumor lysis syndrome (high
givers of need to monitor for emergence
tumor burden).
of anger, aggression, hostility, unusual
changes in mental status. • Avoid tasks ACTION
that require alertness, motor skills until
Targets human epidermal growth factor
response to drug is established (greater
2 (HER2), blocking ligand-initiated in-
risk for dizziness, sleepiness).
tercellular signaling, which can result in
cell growth arrest and cell death. Thera-
peutic Effect: Inhibits cell growth and
pertuzumab metastasis.
per-tue-zue-mab PHARMACOKINETICS
(Perjeta) Peak plasma concentration reached after
j BLACK BOX ALERT j Can result first maintenance dose. Half-life: 18
in embryo-fetal death, birth defects. days.
Pts must be made aware of danger to
P fetus, need for effective contracep- LIFESPAN CONSIDERATIONS
tion. May result in cardiac failure. As-
sess left ventricular ejection fraction. Pregnancy/Lactation: May cause
embryo-fetal harm. Females of repro-
uCLASSIFICATION ductive potential must use effective
PHARMACOTHERAPEUTIC: HER2 contraception during treatment and
receptor antagonist. Monoclonal anti- for at least 7 mos after discontinuation.
body. CLINICAL: Antineoplastic. Unknown if distributed in breast milk.
However, human immunoglobulin G
(IgG) is present in breast milk and
USES is known to cross the placenta. Chil-
Treatment of HER2-positive metastatic dren: Safety and efficacy not estab-
breast cancer in pts who have not re- lished. Elderly: No age-related pre-
ceived prior anti-HER2 therapy or cautions noted.
chemotherapy for metastatic disease
in combination with trastuzumab and INTERACTIONS
DOCEtaxel. Neoadjuvant treatment of pts DRUG: May increase levels of belimumab.
with HER2-positive, locally advanced in- HERBAL: None significant. FOOD: None
flammatory, or early-stage breast cancer known. LAB VALUES: May decrease Hgb,
in combination with trastuzumab and Hct, leukocytes, neutrophils.
DOCEtaxel. Adjuvant treatment of HER2-
positive early breast cancer at high risk of AVAILABILITY (Rx)
recurrence (in combination with trastu- Injection Solution: 420 mg/14 mL (30
zumab and chemotherapy). mg/mL) vial.

underlined – top prescribed drug


pertuzumab 931

ADMINISTRATION/HANDLING cycles. May be administered as one of the


following regimens: 4 preoperative cycles
IV
of pertuzumab, trastuzumab, DOCEtaxel,
Reconstitution • Visually inspect vial then 3 postoperative cycles of 5-fluoro-
for particulate matter or discoloration. uracil, epiRUBicin, and cyclophospha-
Do not use if solution is cloudy, discol- mide (FEC) or 3 or 4 preoperative cycles
ored, or if visible particles are ob- of FEC alone, then 3 or 4 preoperative
served. • Withdraw dose from vial and cycles of pertuzumab, trastuzumab,
dilute into 250 mL 0.9% NaCl only (do DOCEtaxel or 6 preoperative cycles of
not use D5W). • Mix by gentle inver- pertuzumab, trastuzumab, DOCEtaxel,
sion. • Do not shake. and CARBOplatin or 4 preoperative cycles
Rate of administration • Initial dose of dose-dense DOXOrubicin and cyclo-
to be infused over 60 min. • Subse- phosphamide alone, then 4 preopera-
quent doses may be infused over 30–60 tive cycles of pertuzumab, trastuzumab,
min. and PACLitaxel. Note: Continue trastu-
Storage • Refrigerate unused vials. zumab postoperatively to complete 1 yr
Store vials in outside cartons (protects of ­treatment.
from light). • May refrigerate diluted
solution for up to 24 hrs. • Do not Dosage in Renal/Hepatic Impairment
freeze. No dose adjustment.
IV INCOMPATIBILITIES SIDE EFFECTS
Do not mix with any other medications. Frequent (67%–21%): Diarrhea, alopecia,
nausea, fatigue, rash, peripheral neu-
INDICATIONS/ROUTES/DOSAGE ropathy, anorexia, asthenia, mucosal in-
b ALERT c Give as an IV infusion only. flammation, vomiting, peripheral edema,
Do not give by IV push or bolus. myalgia, nail disorder, headache. Occa-
sional (19%–12%): Stomatitis, pyrexia, P
Breast Cancer (Metastatic) dysgeusia, arthralgia, constipation, in-
IV infusion: ADULTS/ELDERLY: Initially, creased lacrimation, pruritus, insomnia,
840 mg given over 60 min, followed by dizziness. Rare (10%–7%): Nasopharyngi-
maintenance dose of 420 mg given over tis, dry skin, paronychia.
30–60 min q3wks until disease progres-
sion or unacceptable toxicity (in combi- ADVERSE EFFECTS/TOXIC
nation with trastuzumab and DOCEtaxel). REACTIONS
Breast Cancer (Adjuvant)
Anemia, leukopenia, neutropenia are
IV infusion: ADULTS, ELDERLY: 840 mg expected responses to therapy, but more
over 60 min, followed by maintenance severe reactions including febrile neu-
dose of 420 mg over 30–60 min q3wks for tropenia may be life-threatening. Upper
a total of 1 yr (up to 18 cycles) or until dis- respiratory tract infection occurs in 17%
ease progression or unacceptable toxicity of pts. Pleural effusion occurred in 5%
(as part of combination regimen contain- of pts. Tumor lysis syndrome may pres-
ing trastuzumab and standard anthracy- ent as acute renal failure, hypocalcemia,
cline- and/or taxane-based therapy). Per- hyperuricemia, hyperphosphatemia.
tuzumab and trastuzumab should begin on Immunogenicity (auto-pertuzumab anti-
day 1 of the first taxane-containing cycle. bodies) reported in 3% of pts. Decreases
in LVEF occurred in 4% of pts. Prior
Breast Cancer (Neoadjuvant) treatment with anthracyclines, chest ra-
IV infusion: ADULTS, ELDERLY: 840 mg diotherapy may further increase risk of
once, followed by 420 mg q3wks for 3–6 decreased LVEF.

Canadian trade name Non-Crushable Drug High Alert drug


932 PHENobarbital

NURSING CONSIDERATIONS palpitations, seizures, vomiting.


• Avoid pregnancy. • Use effective
BASELINE ASSESSMENT contraception, including condoms,
Obtain CBC. Assess left ventricular ejec- during treatment and for at least 7
tion fraction (LVEF) before initiating mos after last dose. • Do not breast-
therapy. Negative pregnancy test must be feed. • Alopecia is reversible, but
confirmed before initiating treatment. new hair growth may have different
Obtain HER2 testing by an FDA-approved color, texture.
laboratory. Screen for active infection.
Offer emotional support.
INTERVENTION/EVALUATION PHENobarbital
Monitor ANC, CBC periodically. Assess
LVEF at regular intervals. Monitor for fee-noe-bar-bi-tal
symptoms of left ventricular dysfunction Do not confuse PHENobarbital
(arrhythmia, cough, dyspnea, peripheral with pentobarbital, Phenergan,
edema). Monitor for infusion reactions, or phenytoin.
hypersensitivity reactions, anaphylaxis.
If a significant infusion reaction occurs, FIXED-COMBINATION(S)
slow or interrupt infusion and administer Donnatal: PHENobarbital/atropine
appropriate medical treatment. Observe (an anticholinergic)/hyoscyamine (an
pt closely for 60 min after the first in- anticholinergic)/scopolamine (an
fusion and for 30 min after subsequent anticholinergic): 16.2 mg/0.0194
infusions. Offer antiemetics if nausea mg/0.1037 mg/0.0065 mg.
occurs. Monitor for symptoms of tumor
lysis syndrome (acute renal failure, hy- uCLASSIFICATION
pocalcemia, hyperuricemia, hyperphos- PHARMACOTHERAPEUTIC: Barbitu-
P phatemia). rate (Schedule IV). CLINICAL: Anti-
PATIENT/FAMILY TEACHING
convulsant.
• Treatment may depress your im-
mune system response and reduce
your ability to fight infection. Report USES
symptoms of infection such as body Management of generalized tonic-clonic
aches, chills, cough, fatigue, fever. (grand mal) seizures, partial seizures,
Avoid those with active infec- control of acute seizure episodes (sta-
tion. • Report symptoms of bone tus epilepticus). OFF-LABEL: Treatment
marrow depression such as bruising, of alcohol withdrawal, sedative/hypnotic
fatigue, fever, shortness of breath, withdrawal.
weight loss; bleeding easily, bloody
urine or stool. • New-onset left heart PRECAUTIONS
dysfunction may occur; report short- Contraindications: Hypersensitivity to
ness of breath, cough, swelling of an- PHENobarbital, other barbiturates, por-
kles or feet, palpitations. • Therapy phyria, dyspnea or airway obstruction,
may cause life-threatening tumor lysis use in nephritic pts (large doses), severe
syndrome (a condition caused by the hepatic impairment. Pts with history of
rapid breakdown of cancer cells), sedative/hypnotic addiction. Intra-arterial
which can cause kidney failure. Report or SQ administration. Cautions: Renal/
decreased urination, amber-colored hepatic impairment, acute/chronic pain,
urine; confusion, difficulty breathing, depression, suicidal tendencies, history
fatigue, fever, muscle or joint pain, of drug abuse, elderly pts, debilitated pts,

underlined – top prescribed drug


PHENobarbital 933
children, hemodynamically ­unstable pts, effect. May decrease concentration/effect
hypoadrenalism, respiratory disease. of dolutegravir, tenofovir, voricon-
azole. HERBAL: Herbals with seda-
ACTION tive properties (e.g., chamomile,
Depresses sensory cortex, decreases kava kava, valerian) may increase CNS
motor activity, alters cerebellar func- depression. FOOD: None known. LAB
tion. Therapeutic Effect: Induces VALUES: May decrease serum bilirubin.
drowsiness, sedation, anticonvulsant Therapeutic serum level: 10–40 mcg/
activity. mL; toxic serum level: greater than 40
mcg/mL.
PHARMACOKINETICS
AVAILABILITY (Rx)
Route Onset Peak Duration 20 mg/5 mL. Oral Solution: 20
Elixir:
PO 20–60 N/A 6–10 hrs mg/5 mL. Injection Solution: 65 mg/mL,
min 130 mg/mL. Tablets: 15 mg, 30 mg, 60
IV 5 min 30 min 4–10 hrs
mg, 100 mg.
Well absorbed after PO, parenteral ad- ADMINISTRATION/HANDLING
ministration. Protein binding: 20%–45%.
IV
Rapidly and widely distributed. Me-
tabolized in liver. Primarily excreted in Reconstitution • May give undiluted
urine. Removed by hemodialysis. Half- or may dilute with NaCl.
life: 53–140 hrs. Rate of administration • Adequately
hydrate pt before and immediately after
LIFESPAN CONSIDERATIONS drug therapy (decreases risk of adverse
Pregnancy/Lactation: Readily crosses renal effects). • Do not inject IV faster
placenta. Distributed in breast milk. Pro- than 30 mg/min for children and 60 mg/
duces respiratory depression in neonates min for adults. Too-rapid IV may produce P
during labor. May cause postpartum severe hypotension, marked respiratory
hemorrhage, hemorrhagic disease in depression. • Inadvertent intra-arterial
newborn. Withdrawal symptoms may ap- injection may result in arterial spasm with
pear in neonates born to women receiv- severe pain, tissue necrosis. Extravasation
ing barbiturates during last trimester of in SQ tissue may produce redness, ten-
pregnancy. Lowers serum bilirubin in ne- derness, tissue necrosis.
onates. Children: May cause paradoxi- Storage • Store vials at room temper-
cal excitement. Elderly: May exhibit ature.
excitement, confusion, mental depres-
sion. Use caution. IM
• Do not inject more than 5 mL in any
INTERACTIONS one IM injection site (produces tissue
DRUG: Alcohol, other CNS depres- irritation). • Inject deep IM into large
sants (e.g., LORazepam, morphine) muscle mass.
may increase CNS depression. May de-
crease effects of warfarin, oral contra- PO
ceptives. Valproic acid may increase • Give without regard to food. • Tab-
concentration, risk of toxicity. Strong lets may be crushed. • Elixir may be
CYP2C19 inducers (e.g., carBAM- mixed with water, milk, fruit juice.
azepine, rifAMPin) may decrease IV INCOMPATIBILITIES
concentration/effect. Strong CYP2C19
inhibitors (e.g., FLUoxetine, fluvox- Amphotericin B complex (Abelcet, AmBi-
aMINE) may increase concentration/ some, Amphotec).

Canadian trade name Non-Crushable Drug High Alert drug


934 phenylephrine

IV COMPATIBILITIES NURSING CONSIDERATIONS


Calcium gluconate, enalapril (Vasotec),
BASELINE ASSESSMENT
fosphenytoin (Cerebyx), propofol (Di-
privan). Assess B/P, pulse, respirations immediately
before administration. Hypnotic: Raise
INDICATIONS/ROUTES/DOSAGE bed rails, provide environment conducive
Status Epilepticus to sleep (back rub, quiet environment, low
IV: ADULTS, ELDERLY, CHILDREN:15 mg/kg lighting). Seizures: Review history of sei-
as a single dose. CHILDREN: 15–20 mg/ zure disorder (length, presence of auras,
kg (Maximum: 1,000 mg) over 10 min; LOC). Observe for recurrence of seizure
may repeat after 15 min (Maximum: activity. Initiate seizure precautions.
40 mg/kg). INTERVENTION/EVALUATION
Seizure Control (Maintenance) Monitor CNS status, seizure activity, he-
Note: Maintenance dose usually starts patic/renal function, respiratory rate,
12 hrs after loading dose. heart rate, B/P. Monitor for therapeutic
PO, IV: ADULTS, ELDERLY, CHILDREN OLDER serum level. Neurologic assessments may
THAN 12 YRS: 2 mg/kg/day in divided doses. be inaccurate until drug has properly
CHILDREN 5–12 YRS: 4–6 mg/kg/day in di- cleared the body. Therapeutic serum
vided doses. CHILDREN 1–5 YRS: 6–8 mg/ level: 10–40 mcg/mL; toxic serum
kg/day in divided doses. CHILDREN YOUNGER level: greater than 40 mcg/mL.
THAN 1 YR: 5–6 mg/kg/day in 1–2 divided
PATIENT/FAMILY TEACHING
doses. NEONATES: 3–4 mg/kg/day given
once daily. • Avoid alcohol, limit caffeine. • May
be habit-forming. • Do not discontinue
Dosage in Renal/Hepatic Impairment abruptly. • May cause dizziness/drows-
No dose adjustment. iness; avoid tasks that require alertness,
P motor skills until response to drug is es-
SIDE EFFECTS tablished.
Occasional (3%–1%): Drowsiness. Rare
(less than 1%): Confusion, paradoxical
CNS reactions (hyperactivity, anxiety in phenylephrine
children; excitement, restlessness in el-
derly, generally noted during first 2 wks of fen-il-ef-rin
therapy, particularly in presence of uncon- (AK-Dilate, Mydfrin, Neo-Syneph-
trolled pain). rine, Sudafed PE)
ADVERSE EFFECTS/TOXIC j BLACK BOX ALERT j Intrave-
nous use should be administered
REACTIONS by adequately trained individuals
Abrupt withdrawal after prolonged therapy familiar with its use.
may produce increased dreaming, night- Do not confuse Mydfrin with Mid-
mares, insomnia, tremor, diaphoresis, rin, or Sudafed PE with Sudafed.
vomiting, hallucinations, delirium, sei-
uCLASSIFICATION
zures, status epilepticus. Skin eruptions
appear as hypersensitivity reaction. Blood PHARMACOTHERAPEUTIC: Alpha-
dyscrasias, hepatic disease, hypocalcemia adrenergic agonist. CLINICAL: Nasal
occur rarely. Overdose produces cold/ decongestant, mydriatic, vasopressor.
clammy skin, hypothermia, severe CNS
depression, cyanosis, tachycardia, Cheyne- USES
Stokes respirations. Toxicity may result in
Nasal decongestant: Topical appli-
severe renal impairment.
cation to nasal mucosa reduces nasal
underlined – top prescribed drug
phenylephrine 935
secretion, promoting drainage of sinus INTERACTIONS
secretions. Parenteral: Vascular failure DRUG: Linezolid, MAOIs (e.g.,
in shock, supraventricular tachycardia, phenelzine, selegiline) may increase
hypotension. vasopressor effects. Tricyclic anti-
PRECAUTIONS depressants (e.g., amitriptyline,
doxepin) may increase vasopressor ef-
Contraindications: Hypersensitivity to fect. Ergot derivatives (e.g., ergota-
phenylephrine. Injection: Severe hy- mine) may increase hypertensive effect.
pertension, ventricular tachycardia. HERBAL: None significant. FOOD: None
Oral: Use within 14 days of MAOI ther- known. LAB VALUES: None significant.
apy. Cautions: Injection: Elderly, hyper-
thyroidism, bradycardia, partial heart AVAILABILITY (OTC)
block, cardiac disease, HF, cardiogenic Injection, Solution: 10 mg/mL. Solution,
shock, hypertension. Oral: Asthma, Nasal Drops (Neo-Synephrine): 0.125%,
bowel obstruction, cardiac disease, 0.25%. Solution, Nasal Spray (Neo-Syn-
ischemic heart disease, hypertension, ephrine): 0.25%, 0.5%. Solution, Oral: 2.5
increased intraocular pressure, elderly, mg/5 mL. Tablets (Sudafed PE): 10 mg.
prostatic hyperplasia.
ACTION ADMINISTRATION/HANDLING
Acts on alpha-adrenergic receptors of IV
vascular smooth muscle. Causes vaso-
constriction of arterioles of nasal mu- Reconstitution • For IV push, dilute
cosa/conjunctiva; produces systemic with NS to a concentration of 0.1–1 mg/mL.
arterial vasoconstriction. Therapeutic • For IV infusion, dilute 10–100 mg
Effect: Decreases mucosal blood flow, with 500 mL 0.9% NaCl or D5W.
relieves congestion. Increases B/P. Re- Rate of administration • For IV
duces heart rate due to decrease in car- push, give over 20–30 sec. • For IV
infusion, titrate dose to maintain systolic P
diac output.
B/P greater than 90 mm Hg.
PHARMACOKINETICS Storage • Store vials at room temper-
ature.
Route Onset Peak Duration
IV Immediate N/A 15–20 min Nasal
IM 10–15 min N/A 0.5–2 hrs • Instruct pt to blow nose prior to admin-
SQ 10–15 min N/A 1 hr istering medication. • With head tilted
back, apply drops in 1 nostril. Wait 5 min
Minimal absorption after intranasal, oph- before applying drops in other nos-
thalmic administration. Metabolized in tril. • Sprays should be administered
liver, GI tract. Primarily excreted in urine. into each nostril with head erect. • Pt
Half-life: 2.5 hrs. should sniff briskly while squeezing con-
tainer, then wait 3–5 min before blowing
LIFESPAN CONSIDERATIONS nose gently. • Rinse tip of spray bottle.
Pregnancy/Lactation: Crosses pla-
centa. Distributed in breast milk. Chil- IV INCOMPATIBILITIES
dren: May exhibit increased absorption, Furosemide (Lasix).
toxicity with nasal preparation. No age-
related precautions noted with systemic IV COMPATIBILITIES
use. Elderly: More likely to experience Amiodarone (Cordarone), dexmedeto-
adverse effects. midine (Precedex), DOBUTamine (Do-

Canadian trade name Non-Crushable Drug High Alert drug


936 phenytoin
butrex), lidocaine, potassium chloride, depression, seizures. Prolonged nasal
propofol (Diprivan), vasopressin. use may produce chronic swelling of
nasal mucosa, rhinitis. If phenyleph-
INDICATIONS/ROUTES/DOSAGE rine 10% ophthalmic is instilled into
Nasal Decongestant denuded/damaged corneal epithelium,
b ALERT c Do not use for more than 3 corneal clouding may result.
days.
Intranasal: ADULTS,ELDERLY, CHIL- NURSING CONSIDERATIONS
DREN 12 YRS AND OLDER: 2–3 drops BASELINE ASSESSMENT
or 2–3 sprays of 0.25%–0.5% solu-
tion into each nostril q4h as needed. Obtain baseline symptomology, vital
CHILDREN 6–11 YRS: 2–3 drops or 2–3
signs. Question history of hypertension,
sprays of 0.25% solution into each nos- cardiac disease, asthma, recent use of
tril q4h as needed. CHILDREN 2–5 YRS: 1 MAOI therapy.
drop of 0.125% solution (dilute 0.5% INTERVENTION/EVALUATION
solution with 0.9% NaCl to achieve Monitor B/P, heart rate. For severe hypo-
0.125%) in each nostril. Repeat q2–4h tension or shock states, monitor central
as needed. venous pressure noninvasive hemody-
PO: ADULTS, ELDERLY, CHILDREN 13 YRS namic monitoring systems.
AND OLDER: 10 mg q4h as needed for
up to 7 days. Maximum: 60 mg/day. PATIENT/FAMILY TEACHING
CHILDREN 6–11 YRS: 5 mg q4h as needed • Discontinue drug if adverse reactions
for up to 7 days. Maximum: 30 mg/ occur. • Do not use for nasal deconges-
day. CHILDREN 4–5 YRS: 2.5 mg q4h as tion for longer than 3 days (rebound con-
needed for up to 7 days. Maximum: 15 gestion). • Discontinue drug if insomnia,
mg/day. dizziness, weakness, tremor, palpitations
occur. • Nasal: Stinging/burning of nasal
P Hypotension, Shock mucosa may occur. • Ophthalmic: Blur-
IV infusion: ADULTS, ELDERLY: 0.5–6 ring of vision with eye instillation generally
mcg/kg/min. Titrate to desired response. subsides with continued therapy. • Dis-
CHILDREN: Initially, 0.1–0.5 mcg/kg/min. continue medication if redness/swelling of
Titrate to desired effect. eyelids, itching occurs.
SIDE EFFECTS
Frequent: Nasal: Rebound nasal con-
gestion due to overuse, esp. when used phenytoin
longer than 3 days. Occasional: Mild
CNS stimulation (restlessness, nervous- fen-i-toyn
ness, tremors, headache, insomnia, (Dilantin, Novo-Phenytoin ,
particularly in those hypersensitive to Phenytek)
sympathomimetics, such as elderly pts). j BLACK BOX ALERT jDo not ex-
Nasal: Stinging, burning, drying of nasal ceed IV rate of 50 mg/min in adults
mucosa. and 1–3 mg/kg/min in pediatric pts.
Do not confuse Dilantin with
ADVERSE EFFECTS/TOXIC Dilaudid or dilTIAZem, or
REACTIONS phenytoin with phenelzine or
Large doses may produce tachycardia, fosphenytoin.
palpitations (particularly in pts with uCLASSIFICATION
cardiac disease), dizziness, nausea,
vomiting. Overdose in pts older than PHARMACOTHERAPEUTIC: Hydan-
60 yrs may result in hallucinations, CNS toin. CLINICAL: Anticonvulsant.

underlined – top prescribed drug


phenytoin 937

USES features; excess body hair. Elderly: No


Management of generalized tonic-clonic age-related precautions noted but lower
seizures (grand mal), complex partial dosages recommended.
seizures, status epilepticus. Prevention
INTERACTIONS
of seizures following head trauma/neu-
rosurgery. OFF-LABEL: Prevention of early DRUG: Alcohol, other CNS depres-
post-traumatic seizures following trau- sants (e.g., LORazepam, mor-
matic brain injury. phine, zolpidem) may increase
CNS depression. Amiodarone, ci-
PRECAUTIONS metidine, disulfiram, FLUoxetine,
Contraindications: Hypersensitivity to isoniazid, sulfonamides may in-
phenytoin, other hydantoins. Concur- crease concentration/effects, risk
rent use of delavirdine. History of acute of toxicity. May decrease effects of
phenytoin therapy–induced hepatotoxic- glucocorticoids (e.g., dexametha-
ity. IV (additional): Second- and third- sone, predniSONE), oral contra-
degree AV block, sinoatrial block, sinus ceptives. Lidocaine, propranolol
bradycardia, Adams-Stokes syndrome. may increase cardiac depressant ef-
Cautions: Porphyria, diabetes, renal/ fects. Valproic acid may decrease
hepatic impairment, pts at increased risk metabolism, increase concentration.
of suicidal behavior/thoughts, elderly/ May decrease concentration/effect of
debilitated pts, low serum albumin, car- apixaban, axitinib, dabigatran,
diac disease, hypothyroidism, pts of Asian dronedarone, itraconazole, iv-
descent. abradine, niMODipine, rivaroxa-
ban. HERBAL: Herbals with seda-
ACTION tive properties (e.g., chamomile,
Stabilizes neuronal membranes in mo- kava kava, valerian) may increase
tor cortex. Decreases influx of sodium CNS depression. FOOD: None known.
during generation of nerve impulses. LAB VALUES: May increase serum P
Therapeutic Effect: Decreases seizure glucose, GGT, alkaline phosphatase.
activity. Therapeutic serum level: 10–20
mcg/mL; toxic serum level: greater
PHARMACOKINETICS than 20 mcg/mL.
Slowly, variably absorbed after PO ad-
AVAILABILITY (Rx)
ministration. Protein binding: 90%–95%.
Widely distributed. Metabolized in liver. Capsules, Extended-Release: 30 mg, 100
Primarily excreted in urine. Not removed mg, 200 mg, 300 mg. Injection Solu-
by hemodialysis. Half-life: 7–42 hrs. tion: 50 mg/mL. Suspension, Oral: 125
mg/5 mL. Tablets, Chewable: 50 mg.
LIFESPAN CONSIDERATIONS
ADMINISTRATION/HANDLING
Pregnancy/Lactation: Crosses pla-
centa; distributed in small amount in IV
breast milk. Fetal hydantoin syndrome
(craniofacial abnormalities, nail/digital b ALERT c Give by IV push or IV pig-
hypoplasia, prenatal growth deficiency) gyback. IV push can be painful (chemical
has been reported. Increased frequency irritation of vein due to alkalinity of solu-
of seizures in pregnant women due to tion). To minimize effect of irritation,
altered absorption of metabolism of phe- flush IV with sterile saline after dose is
nytoin. May increase risk of hemorrhage administered.
in neonate, maternal bleeding during Reconstitution • May give undiluted
delivery. Children: More susceptible to or may dilute with 0.9% NaCl to a con-
gingival hyperplasia, coarsening of facial centration of 5 mg/mL or more.
Canadian trade name Non-Crushable Drug High Alert drug
938 phenytoin
Rate of administration • Administer PO: ADULTS, ELDERLY: Loading Dose:
at rate not exceeding 50 mg/min in 1 g divided into 3 doses given at 2-hr
adults, 20 mg/min in elderly, pts with intervals. Maintenance (begins 24
preexisting cardiovascular conditions. In hrs after loading dose): Initially 100
neonates, administer at rate not exceed- mg 3 times/day; adjust at no less than
ing 1–3 mg/kg/min. • Infuse diluted 7–10-day intervals. Usual dose: 100
solutions using an in-line filter. • Se- mg 3–4 times/day up to 200 mg 3
vere hypotension, cardiovascular col- times/day (may consider 300 mg once
lapse occur if rate of IV injection exceeds daily in pts established on 100 mg 3
50 mg/min for adults. • IV toxicity times/day). CHILDREN: Initially, 5 mg/
characterized by CNS depression, cardio- kg/day in 2–3 divided doses. Adjust
vascular collapse. dose at 7- to 10-day intervals. Main-
Storage • Precipitate may form if tenance: 4–8 mg/kg/day. Maximum:
parenteral form is refrigerated (will dis- 300 mg/day.
solve at room temperature). • Slight
yellow discoloration of parenteral form Dosage in Renal/Hepatic Impairment
does not affect potency, but do not use if No dose adjustment.
solution is cloudy or precipitate forms.
Discard if not used within 4 hrs of SIDE EFFECTS
preparation. Frequent: Drowsiness, lethargy, confu-
sion, slurred speech, irritability, gingi-
PO val hyperplasia, hypersensitivity reac-
• Give with food if GI distress occurs. tion (fever, rash, lymphadenopathy),
• Tablets may be chewed. • Shake oral constipation, dizziness, nausea. Occa-
suspension well before using. • Separate sional: Headache, hirsutism, coarsen-
administration of phenytoin with antacids ing of facial features, insomnia, muscle
or tube feeding by 2 hrs. twitching.
P
IV INCOMPATIBILITIES ADVERSE EFFECTS/TOXIC
DilTIAZem (Cardizem), DOBUTamine REACTIONS
(Dobutrex), enalapril (Vasotec), hepa- Abrupt withdrawal may precipitate
rin, HYDROmorphone (Dilaudid), insu- status epilepticus. Blood dyscrasias,
lin, lidocaine, morphine, nitroglycerin, osteomalacia (due to interference of
norepinephrine (Levophed), potassium vitamin D metabolism) may occur.
chloride, propofol (Diprivan). Toxic phenytoin blood concentration
(25 mcg/mL or more) may produce
INDICATIONS/ROUTES/DOSAGE ataxia, nystagmus, diplopia. As level
Status Epilepticus
increases, extreme lethargy to coma-
IV: ADULTS, ELDERLY, ADOLESCENTS:
tose state occurs. May increase risk of
Loading dose: 20 mg/kg at maximum suicidal thoughts and behavior. Severe
rate of 25–50 mg/min. May repeat in 10 cutaneous reactions including toxic
min after loading dose with dose of 5–10 epidermal necrolysis, Stevens-Johnson
mg/kg. INFANTS, CHILDREN: Loading syndrome may occur. Life-threatening
dose: 20 mg/kg at maximum rate of 1 drug reaction with eosinophilia and
mg/kg/min. May give additional dose of systemic symptoms (DRESS) (multi-
5–10 mg/kg after loading dose. organ hypersensitivity) may present as
lymphadenopathy, fever, facial swell-
Seizure Control (Maintenance)
ing, hepatitis, nephritis, myocarditis,
Note: Loading dose not used in pts with myositis. Hepatotoxicity, acute hepatic
history of renal/hepatic disease. failure were reported.

underlined – top prescribed drug


phosphates p­ otassium sodium 939

NURSING CONSIDERATIONS (may precipitate seizures). • Strict


maintenance of drug therapy is essential
BASELINE ASSESSMENT for seizure control, arrhyth-
Anticonvulsant: Review history of mias. • Avoid alcohol. • Report
seizure disorder (intensity, frequency, changes in behavior, thoughts of sui-
duration, LOC). Initiate seizure precau- cide.
tions. LFT, CBC should be performed
before beginning therapy and periodi-
cally during therapy. Repeat CBC 2 wks
following initiation of therapy and 2 phosphates
wks following administration of mainte-
nance dose. ­potassium sodium
INTERVENTION/EVALUATION fos-fates
Observe frequently for recurrence of
uCLASSIFICATION
seizure activity. Monitor ECG for cardiac
arrhythmia. Assess for clinical improve- PHARMACOTHERAPEUTIC: Electro-
ment (decrease in intensity/frequency of lyte supplement. CLINICAL: Mineral.
seizures). Monitor for signs/symptoms of
depression, suicidal tendencies, unusual
behavior. Monitor CBC with differential, USES
renal function, LFT, B/P (with IV use).
Prevention and treatment of hypophos-
Assist with ambulation if drowsiness,
phatemia.
lethargy occurs. Monitor for suicidal
ideation or behaviors. Monitor for thera- PRECAUTIONS
peutic serum level (10–20 mcg/mL).
Contraindications: K-phosphate:
Therapeutic serum level: 10–20 mcg/
Hyperkalemia, hyperphosphatemia,
mL; toxic serum level: greater than 20
hypocalcemia. Na-phosphate: Hy- P
mcg/mL. Free unbound levels: Thera-
pocalcemia, hypernatremia, hyperpho-
peutic: 1–2 mcg/mL; toxic: more than
sphatemia. Cautions: Renal impairment,
2 mcg/mL.
concomitant use of potassium-sparing
PATIENT/FAMILY TEACHING drugs, acid-base alteration, digitalized
• Pain may occur with IV injec- pts, cardiac disease, metabolic alkalo-
tion. • To prevent gingival hyperplasia sis.
(bleeding, tenderness, swelling of
ACTION
gums), maintain good oral hygiene,
gum massage, regular dental vis- Active in bone deposition, calcium
its. • Serum levels should be per- metabolism, utilization of B complex
formed every mo for 1 yr after mainte- vitamins. Act as buffers in maintaining
nance dose is established and q3mos acid-base balance. Exert osmotic effect
thereafter. • Report sore throat, fever, in small intestine. Therapeutic Ef-
glandular swelling, skin reaction (he- fect: Correct hypophosphatemia, acidify
matologic toxicity). • Drowsiness urine, prevent calcium deposits in uri-
usually diminishes with continued ther- nary tract, promote peristalsis in GI tract.
apy. • Avoid tasks that require alert-
PHARMACOKINETICS
ness, motor skills until response to drug
is established. • Do not abruptly with- Poorly absorbed after PO administration.
draw medication after long-term use PO form excreted in feces; IV form ex-
creted in urine.

Canadian trade name Non-Crushable Drug High Alert drug


940 phosphates ­potassium sodium

LIFESPAN CONSIDERATIONS INDICATIONS/ROUTES/DOSAGE


Pregnancy/Lactation: Use caution Note: (K-Phosphate): For each
in pregnant women with other medical mmol of phosphate, 1.5 mEq of K will
conditions (e.g., preeclampsia). Chil- be given. (Na-Phosphate): For each
dren: Increased risk of dehydration in mmol of phosphate, 1.3 mEq of Na will
pts younger than 12 yrs. Elderly: No be given.
age-related precautions noted.
Hypophosphatemia
INTERACTIONS (Potassium/Sodium Phosphate):
Phosphate level 2.3–3 mg/dL: 0.16–
DRUG: ACE inhibitors (e.g., enala-
pril, lisinopril), eplerenone, iron 0.32 mmol/kg over 4–6 hr. Phosphate
level 1.6–2.2 mg/dL: 0.32–0.64
salts, magnesium salts, potassium-
containing medications, potassium- mmol/kg over 4–6 hr. Phosphate
level less than 1.5 mg/dL: 0.64–1
sparing diuretics (e.g., spironolac-
tone), salt substitutes containing mmol/kg over 8–12 hr.
potassium phosphate may increase
serum potassium. Antacids, sucralfate SIDE EFFECTS
may decrease absorption. Calcium- Frequent: Mild laxative effect (in first
containing medications may increase few days of therapy). Occasional: Di-
risk of calcium deposition in soft tis- arrhea, nausea, abdominal pain, vom-
sues, decrease phosphate absorption. iting. Rare: Headache, dizziness, con-
HERBAL: None significant. FOOD: None fusion, heaviness of lower extremities,
known. LAB VALUES: None significant. fatigue, muscle cramps, paresthesia,
peripheral edema, arrhythmias, weight
AVAILABILITY (Rx) gain, thirst.
Injection Solution (Potassium Phos-
phate): 3 mmol phosphate and 4.4 mEq ADVERSE EFFECTS/TOXIC
P potassium per mL. Injection Solution (So- REACTIONS
dium Phosphate): 3 mmol phosphate and
4 mEq sodium per mL. Hyperphosphatemia may produce ex-
traskeletal calcification.
ADMINISTRATION/HANDLING
IV NURSING CONSIDERATIONS
Reconstitution • Must be diluted. BASELINE ASSESSMENT
Soluble in all commonly used IV solu- Obtain BMP, serum phosphate, ionized
tions. calcium. Question history of renal im-
Rate of administration • Infuse over
pairment, cardiac disease. Receive full
minimum of 4 hrs (usually over 6 hrs). medication history and screen for inter-
Maximum rate: 0.06 mmol/kg/hr. actions. Assess hydration status.
Storage • Store at room temperature.
INTERVENTION/EVALUATION
IV INCOMPATIBILITIES
Routinely monitor serum calcium,
Amiodarone, DOBUTamine (Dobutrex), phosphorus, potassium, sodium, ALT,
pantoprazole (Protonix). AST, alkaline phosphatase, bilirubin.
IV COMPATIBILITIES PATIENT/FAMILY TEACHING
DilTIAZem (Cardizem), enalapril (Vaso- • Report diarrhea, nausea, vomiting.
tec), famotidine (Pepcid), metoclopramide
(Reglan), niCARdipine (Cardene).

underlined – top prescribed drug


piperacillin/tazobactam 941
unchanged in urine. Removed by he-
piperacillin/ modialysis. Half-life: 0.7–1.2 hrs
tazobactam (increased in hepatic cirrhosis, renal
impairment).
pye-per-a-sil-in/tay-zoe-bak-tam LIFESPAN CONSIDERATIONS
(Zosyn)
Do not confuse Zosyn with Pregnancy/Lactation: Readily crosses
Zofran or Zyvox. placenta; appears in cord blood, amni-
otic fluid. Distributed in breast milk in
uCLASSIFICATION low concentrations. May lead to aller-
PHARMACOTHERAPEUTIC: Penicil- gic sensitization, diarrhea, candidiasis,
lin. CLINICAL: Antibiotic. skin rash in infant. Children: Dos-
age not established for pts younger
than 12 yrs. Elderly: Age-related
renal impairment may require dosage
USES
adjustment.
Treatment of moderate to severe bacte-
rial infections, including community- INTERACTIONS
acquired/nosocomial pneumonia, DRUG: May decrease concentration/
intra-abdominal, pelvic, skin, and skin effects of aminoglycosides (e.g.,
structure infections. Tazobactam expands gentamicin, tobramycin). May
piperacillin activity to include beta-lac- increase concentration, toxicity of
tamase–producing strains of S. aureus, methotrexate. Probenecid may in-
H. influenzae, Bacteroides, PsAg, Aci- crease concentration, risk of toxicity.
netobacter, Klebsiella pneumoniae, E. HERBAL: None significant. FOOD: None
coli. OFF-LABEL: Surgical prophylaxis, known. LAB VALUES: May increase
complicated intra-abdominal infections. serum sodium, alkaline phosphatase,
bilirubin, LDH, ALT, AST, BUN, creati- P
PRECAUTIONS nine, PT, PTT. May decrease serum po-
Contraindications: Hypersensitivity to tassium. May cause positive Coombs’
piperacillin/tazobactam, any penicillin. test.
Cautions: History of allergies (esp. cepha-
losporins, beta-lactamase inhibitors), renal AVAILABILITY (Rx)
impairment, preexisting seizure disorder. b ALERT c Piperacillin/tazobactam is a
combination product in an 8:1 ratio of
ACTION piperacillin to tazobactam. Injection
Piperacillin: Inhibits bacterial cell Powder: 2.25 g, 3.375 g, 4.5 g. Premix
wall synthesis by binding to PCN-binding Ready to Use: 2.25 g (50 mL), 3.375 g
proteins, which inhibit the final step of (50 mL), 4.5 g (100 mL).
peptidoglycan synthesis. Therapeutic
Effect: Bactericidal. Tazobactam: ADMINISTRATION/HANDLING
Inactivates bacterial beta-lactamase. IV
Therapeutic Effect: Protects piperacil-
lin from enzymatic degradation, extends Reconstitution • Reconstitute each 1
its spectrum of activity, prevents bacterial g with 5 mL D5W or 0.9% NaCl. Shake
overgrowth. vigorously to dissolve. • Further dilute
with at least 50 mL D5W or 0.9% NaCl.
PHARMACOKINETICS Rate of administration • Infuse
Protein binding: 16%–30%. Widely over 30 min. Expanded infusion over
distributed. Primarily excreted 3–4 hrs.

Canadian trade name Non-Crushable Drug High Alert drug


942 piperacillin/tazobactam
Storage • Reconstituted vial is stable Dosage for Hemodialysis
for 24 hrs at room temperature or 48 hrs IV: ADULTS, ELDERLY: 2.25 g q12 with
if refrigerated. • After further dilution, additional dose of 0.75 g after each dialysis
stable for 24 hrs at room temperature or session.
7 days if refrigerated. Dosage for CRRT

IV INCOMPATIBILITIES CVVH 2.25–3.375 g q6–8h


CVVHD 2.25–3.375 g q6h
Amphotericin B (Fungizone), amphoteri- CVVHDF 3.375 g q6h
cin B complex (Abelcet, AmBisome, Am-
photec), famotidine (Pepcid), haloperi- Dosage in Renal Impairment
dol (Haldol), hydrOXYzine (Vistaril), Dosage and frequency are modified
vancomycin (Vancocin). based on creatinine clearance.

IV COMPATIBILITIES Dosage in Hepatic Impairment


Bumetanide (Bumex), calcium gluco- No dose adjustment.
nate, dexmedetomidine (Precedex), di-
phenhydrAMINE (Benadryl), DOPamine SIDE EFFECTS
(Intropin), enalapril (Vasotec), furose- Frequent: Diarrhea, headache, con-
mide (Lasix), granisetron (Kytril), hepa- stipation, nausea, insomnia, rash. Oc-
rin, hydrocortisone (Solu-CORTEF), HY- casional: Vomiting, dyspepsia, pruritus,
DROmorphone (Dilaudid), LORazepam fever, agitation, candidiasis, dizziness,
(Ativan), magnesium sulfate, methyl- abdominal pain, edema, anxiety, dyspnea,
PREDNISolone (SOLU-Medrol), metoclo- rhinitis.
pramide (Reglan), morphine, ondanse-
tron (Zofran), potassium chloride. ADVERSE EFFECTS/TOXIC
REACTIONS
INDICATIONS/ROUTES/DOSAGE Antibiotic-associated colitis, other su-
P perinfections (abdominal cramps, se-
Note: Extended Infusion: ADULTS, EL-
DERLY: 3.375–4.5 g over 4 hrs q8h. vere watery diarrhea, fever) may result
from altered bacterial balance in GI
Usual Dosage tract. Overdose, more often with renal
IV: ADULTS, ELDERLY: 4.5 g q6–8h or impairment, may produce seizures, neu-
3.375 g q6h. Maximum: 18 g daily. rologic reactions. Severe hypersensitivity
ADOLESCENTS, CHILDREN, INFANTS: 240– reactions, including anaphylaxis, occur
300 mg piperacillin/kg/day divided in rarely.
3–4 doses. Maximum: 16 g/day. NEO-
NATES: 80–100 mg piperacillin compo- NURSING CONSIDERATIONS
nent/kg/dose q6–8h. BASELINE ASSESSMENT
Creatinine Clearance Dosage Question for history of allergies, esp. to
20–40 mL/min 2.25 g q6h (3.375 g penicillins, cephalosporins. Obtain base-
q6h for nosoco- line CBC with differential, BMP, LFT; uri-
mial pneumonia) nalysis; PT, aPTT (if on anticoagulants or
Less than 20 mL/min 2.25 g q8h (2.25 g history of coagulopathy).
q6h for nosoco-
mial pneumonia) INTERVENTION/EVALUATION
Extended Infusion Monitor daily pattern of bowel activ-
3.375 g q12h ity, stool consistency; mild GI effects
may be tolerable, but increasing

underlined – top prescribed drug


plecanatide 943
severity may indicate onset of an- PHARMACOKINETICS
tibiotic-associated colitis. Be alert Minimal absorption systemically;
for superinfection: fever, vomiting, mainly confined to GI tract. Metabo-
diarrhea, anal/genital pruritus, oral lized within GI tract to active metabo-
mucosal changes (ulceration, pain, lite. Undergoes proteolytic degradation
erythema). Monitor I&O, urinalysis. within intestinal lumen to smaller pep-
Monitor serum electrolytes, esp. po- tides and amino acids. Half-life: Not
tassium, renal function tests. specified.
LIFESPAN CONSIDERATIONS
plecanatide Pregnancy/Lactation: Unknown
if distributed in breast milk. Chil-
ple-kan-a-tide dren: Contraindicated in pts younger
(Trulance) than 6 yrs. Safety and efficacy not es-
j BLACK BOX ALERT jContrain- tablished in pts aged 6 to less than
dicated in pts younger than 6 18 yrs. Severe, possibly fatal, dehy-
yrs due to risk of life-threatening dration may occur in pediatric pts
dehydration and death. Safety younger than 18 yrs due to increased
and efficacy not established in pts
younger than 18 yrs; avoid use. intestinal fluid secretion; avoid use.
Do not confuse plecanatide with Elderly: No age-related precautions
exenatide, lixisenatide, pramlin- noted.
tide or Trulance with Truvada. INTERACTIONS
uCLASSIFICATION DRUG: None known. HERBAL: None sig-
PHARMACOTHERAPEUTIC: Gua- nificant. FOOD: None known. LAB VAL-
nylate cyclase-C agonist. CLINI- UES: May increase serum ALT, AST.
CAL: GI agent. P
AVAILABILITY (Rx)
Tablets: 3 mg.
USES
Treatment of adults with chronic idio- ADMINISTRATION/HANDLING
pathic constipation or irritable bowel PO
syndrome with constipation. • Give with or without food. • If a
dose is missed, skip the dose and give at
PRECAUTIONS next regularly scheduled time; do not
Contraindications: Hypersensitivity to ple- double dose. • Give tablet whole; do
canatide. Pts younger than 6 yrs of age, not break, cut, or divide. • For pts with
mechanical GI obstruction (known or dysphagia, tablet may be crushed and
suspected). Cautions: Dehydration. Avoid mixed in applesauce, or dispersed in 30
use in pts younger than 18 yrs of age. mL of water and given orally or via NG
tube. After administration of dispersed
ACTION tablet, refill container with additional 30
Binds and agonizes guanylate cyclase-C mL of water and give remaining contents.
on luminal surface of intestinal epithe- Flush NG tube with additional 10 mL of
lium, increasing cyclic guanosine mono- water.
phosphate (cGMP), resulting in chloride
and bicarbonate secretion into the intes- INDICATIONS/ROUTES/DOSAGE
tinal lumen. Therapeutic Effect: In- Chronic Idiopathic Constipation, Irritable
creases intestinal fluid and accelerates GI Bowel Syndrome
transit time. PO: ADULTS, ELDERLY: 3 mg once daily.

Canadian trade name Non-Crushable Drug High Alert drug


944 polyethylene glycol
Dosage in Renal/Hepatic Impairment TriLyte)
Not specified; use caution. Do not confuse MiraLax with
Mirapex.
SIDE EFFECTS
Occasional (5%): Diarrhea. Rare (less uCLASSIFICATION
than 2%): Abdominal pain/tenderness, PHARMACOTHERAPEUTIC: Osmotic.
flatulence. CLINICAL: Bowel evacuant, laxative.

ADVERSE EFFECTS/
TOXIC REACTIONS USES
Severe diarrhea reported in less than 1% Polyethylene glycol-electrolyte solu-
of pts; usually occurred within the first 3 tion: Bowel cleansing before GI examina-
days. tion, colon surgery. Polyethylene glycol:
Treatment of occasional constipation.
NURSING CONSIDERATIONS PRECAUTIONS
BASELINE ASSESSMENT Contraindications: Hypersensitivity to poly-
Question characteristics of constipa- ethylene glycol. Bowel perforation, gastric
tion, frequency of bowel movements. retention, GI obstruction, megacolon, toxic
Assess bowel sounds. Assess hydration colitis, toxic ileus. Cautions: Propylene
status. glycol: Renal impairment. Propylene
glycol–electrolyte solution: Ulcerative
INTERVENTION/EVALUATION colitis, dehydration, medications altering
Encourage fluid intake. Monitor daily electrolytes, hyponatremia, cardiac ar-
pattern of bowel activity, stool consis- rhythmias, impaired gag reflex, history of
tency. Monitor for abdominal pain, de- seizures, elderly.
hydration.
P ACTION
PATIENT/FAMILY TEACHING
Induces catharsis by osmotic effect. Thera-
• Report severe diarrhea. • Drink peutic Effect: Alleviates constipation,
plenty of fluids. • Do not take laxatives cleanses bowel without depleting electro-
unless approved by prescriber. • Tab- lytes.
lets may be taken whole, dispersed in
water, or crushed and mixed in apple- PHARMACOKINETICS
sauce. • Securely store tablets away Route Onset Peak Duration
from children; life-threating dehydra- PO (bowel 1–2 hrs N/A N/A
tion may occur if accidentally ingested cleansing)
by children younger than 6 yrs. PO (consti- 2–4 N/A N/A
pation) days

polyethylene glycol LIFESPAN CONSIDERATIONS


Pregnancy/Lactation: Unknown if
drug crosses placenta or is distributed in
polyethylene glycol– breast milk. Children/Elderly: No age-
electrolyte solution related precautions noted.

pol-ee-eth-il-een-glye-kol
(CoLyte, GoLYTELY, Klean-Prep ,
MiraLax, NuLytely, Peglyte ,

underlined – top prescribed drug


pomalidomide 945

INTERACTIONS SIDE EFFECTS


DRUG: None significant. HERBAL: None Frequent (50%): Some degree of ab-
significant. FOOD: None known. LAB dominal fullness, nausea, bloating. Oc-
VALUES: None significant. casional (10%–1%): Abdominal cramp-
ing, vomiting, anal irritation. Rare
AVAILABILITY (Rx) (less than 1%): Urticaria, rhinorrhea,
Powder for Oral Solution: Propylene dermatitis.
glycol: (Miralax): 17 g/dose. Propylene
glycol–electrolyte solution: (CoLyte, Go- ADVERSE EFFECTS/TOXIC
LYTELY): See individual product for spe- REACTIONS
cific ingredients. None known.
ADMINISTRATION/HANDLING NURSING CONSIDERATIONS
PO BASELINE ASSESSMENT
Polyethylene glycol–electrolyte so- Do not give oral medication within 1 hr
lution: • Refrigerate reconstituted of start of therapy (may not adequately be
solutions; use within 48 hrs. • May absorbed before GI cleansing).
use tap water to prepare solution. INTERVENTION/EVALUATION
Shake vigorously for several min to
ensure complete dissolution of pow- Assess bowel sounds for peristalsis.
der. • Fasting should occur for more Monitor daily pattern of bowel activity,
than 3 hrs prior to ingestion of solu- stool consistency. Assess for abdominal
tion (always avoid solid food less than disturbances. Monitor serum electro-
2 hrs prior to administration). • Only lytes.
clear liquids permitted after administra- PATIENT/FAMILY TEACHING
tion. • May give via NG tube. • Rapid • May take 2–4 days to produce a bowel
drinking preferred. Chilled solution is movement. • Report unusual cramps, P
more palatable. bloating, diarrhea.
Polyethylene glycol: • Add to 4- to
8-oz beverage.
INDICATIONS/ROUTES/DOSAGE pomalidomide
Bowel Evacuant
PO: ADULTS, ELDERLY: Before GI ex- poe-ma-lid-oh-mide
amination: 240 mL (8 oz) q10min (Pomalyst)
until 4 L consumed or rectal effluent j BLACK BOX ALERT jMay
clear. NG tube: 20–30 mL/min until 4 cause life-threatening birth defects.
Pregnancy contraindicated.
L given. Exclude pregnancy before initiating
treatment. Females of reproduc-
Constipation tive potential must use two reliable
PO: (Miralax): ADULTS: 17 g or 1 forms of contraception or continu-
heaping tbsp/day. CHILDREN 6 MOS ously abstain during treatment and
AND OLDER: 0.2–0.8 g/kg/day. Maxi- for 4 wks after treatment. Deep vein
mum: 17 g/day. thrombosis and pulmonary embo-
lism may occur. Consider venous
thromboembolism (VTE) prophylaxis
Dosage in Renal/Hepatic Impairment during treatment.
No dose adjustment.

Canadian trade name Non-Crushable Drug High Alert drug


946 pomalidomide
uCLASSIFICATION forms of birth control (intrauterine de-
PHARMACOTHERAPEUTIC: Thalido- vice [IUD], tubal ligation) plus barrier
mide analogue. CLINICAL: Antineo- methods. Avoid pregnancy for at least 4
plastic. wks after discontinuation. Males: Must
use condoms during treatment and up to
1 mo after treatment, despite prior his-
USES tory of vasectomy. Do not donate sperm.
Children: Safety and efficacy not estab-
Treatment of multiple myeloma in pts
who have received at least two prior lished. Elderly: May have increased risk
therapies including lenalidomide and of serious adverse effects, renal failure,
bortezomib and who have demonstrated electrolyte imbalance.
disease progression on or within 60 days INTERACTIONS
of completion of the last therapy.
DRUG: May decrease the therapeutic ef-
PRECAUTIONS fect; increase adverse effects of vaccines
(live). CNS depressants (e.g., alco-
b ALERT c Do not donate blood prod- hol, morphine, zolpidem) may in-
ucts during therapy and for 1 month after crease CNS depression. HERBAL: Herb-
therapy discontinuation; male pts must als with sedative properties (e.g.,
not donate sperm. chamomile, kava kava, valerian) may
Contraindications: Hypersensitivity to increase CNS depression. Echinacea may
pomalidomide. Pregnancy. Cautions: Ane- decrease therapeutic effect. FOOD: None
mia, HF, hepatic/renal impairment, smok- significant. LAB VALUES: May decrease
ing, breastfeeding, or prior history of CVA, Hgb, Hct, neutrophils, platelets, leuko-
MI, DVT, PE. cytes, lymphocytes, serum calcium, po-
ACTION tassium, sodium. May increase serum
calcium, creatinine, glucose.
P Inhibits tumor cell proliferation and
induces apoptosis (cell death) of he- AVAILABILITY (Rx)
matopoietic cells. Enhances T-cell– and Capsules: 1 mg, 2 mg, 3 mg, 4 mg.
natural killer (NK) cell–mediated immu-
nity. Inhibits proinflammatory cytokines. ADMINISTRATION/HANDLING
Therapeutic Effect: Inhibits tumor cell PO
growth and metastasis. • Do not break, crush, or open cap-
PHARMACOKINETICS sule. • Give on empty stomach; must
administer at least 2 hrs before or 2 hrs
Readily absorbed following PO admin- after meal.
istration. Metabolized in liver. Pro-
tein binding: 12%–44%. Peak plasma INDICATIONS/ROUTES/DOSAGE
concentration: 2–3 hrs. Excreted in Note: Absolute neutrophil count (ANC)
urine (73%), feces (15%). Half-life: should be 500 cells/mm3 or greater and
8–10 hrs. platelets 50,000 cells/mm3 or greater
prior to starting new cycles of therapy.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Pregnancy/ Multiple Myeloma
breastfeeding contraindicated. May PO: ADULTS/ELDERLY: 4 mg once daily
cause fetal harm. Unknown if distrib- on days 1–21 of 28-day cycle (in com-
uted in breast milk. Do not breastfeed. bination with dexamethasone). Continue
Must verify negative pregnancy status until disease progression or unaccept-
before initiation. Must use two reliable able toxicity.

underlined – top prescribed drug


pomalidomide 947
Dose Modification expected outcome of therapy; may in-
Neutropenia crease risk of infection such as pneu-
ANC less than 500 cells/mm3 or fe- monia, upper respiratory tract infec-
brile neutropenia: Interrupt treatment tion, UTI. Neurologic events such as
until ANC is greater than 500 cells/mm3, acute confusion, dizziness reported.
then reduce dose to 3 mg once daily. Any Peripheral neuropathy occurred in
subsequent drop of ANC less than 18% of pts. Venous thromboembolism
500 cells/mm3 after prior reduc- including DVT, PE occurred in 3% of
tion: Interrupt treatment until ANC is pts. Epistaxis occurred in 15% of pts.
greater than 500 cells/mm3, then reduce Increased risk of secondary malig-
dose at 1 mg less than previous dose. Dis- nancies reported. Acute renal failure
continue if 1-mg dose is intolerable. reported in 16% of pts. Additional
Thrombocytopenia adverse events may include interstitial
Platelet count less than 25,000 cells/ lung disease (ILD), neutropenic sepsis,
mm3: Interrupt treatment until platelet Pneumocystis jiroveci pneumonia, re-
count greater than 50,000 cells/mm3, then spiratory syncytial virus infection, uri-
reduce dose to 3 mg once daily. Any subse- nary retention, vertigo.
quent platelet drop to less than 25,000
cells/mm3: Interrupt treatment until plate- NURSING CONSIDERATIONS
let count greater than 50,000 cells/mm3, BASELINE ASSESSMENT
then reduce dose at 1 mg less than previous
dose. Discontinue if 1-mg dose is intolerable. Obtain vital signs, CBC with differential,
serum chemistries, esp. magnesium,
Dosage in Renal Impairment phosphate, ionized calcium, PT/INR,
Avoid use in pts with serum creatinine more urinalysis. Confirm negative pregnancy
than 3 mg/dL or CrCl less than 45 mL/min. status 10–14 days before and 24 hrs
before starting treatment. Receive full
Dosage in Hepatic Impairment medication history. Obtain baseline P
Avoid use with bilirubin more than 2 mg/ neurologic exam. Question history of
dL and ALT, AST more than 3 times upper diabetes mellitus, electrolyte imbal-
limit of normal (ULN). ance, hepatic/renal impairment, pul-
monary disease, thromboembolism,
SIDE EFFECTS smoking.
Frequent (55%–22%): Fatigue, constipa- INTERVENTION/EVALUATION
tion, nausea, diarrhea, dyspnea, back Monitor CBC, serum chemistries, PT/
pain, peripheral edema, musculoskeletal INR. Offer antiemetics for nausea, vomit-
chest pain, anorexia, rash. Occasional ing. Monitor pregnancy status every mo
(20%–7%): Dizziness, pyrexia, muscle
during treatment and for at least 4 mos
spasms, arthralgia, pruritus, vomiting, after discontinuation. Obtain ECG for
cough, weight loss, headache, bone pain, palpitations, chest pain, hypokalemia,
muscular weakness, anxiety, musculo- hyperkalemia, hypocalcemia, bradycar-
skeletal pain, peripheral neuropathy, dia, ventricular arrhythmias. Immediately
chills, dry skin, tremor, insomnia. Rare report dyspnea, chest pain, hypoxia, uni-
(6%–1%): Hyperhidrosis, extremity pain,
lateral peripheral edema/pain (may indi-
back pain, night sweats, constipation. cate thromboembolic event). Consider
sequential compression device (SCD) for
ADVERSE EFFECTS/TOXIC immobilized pts. Perform routine neuro-
REACTIONS logic assessments to screen for confusion,
Myelosuppression (neutropenia, leu- delirium. Monitor urine output, fre-
kopenia, thrombocytopenia) is an quency.

Canadian trade name Non-Crushable Drug High Alert drug


948 ponatinib
PATIENT/FAMILY TEACHING USES
• May cause birth defects or miscarriage. Treatment of pts with chronic, acceler-
Do not breastfeed. Consult with gynecolo- ated, or blast phase chronic myeloid
gist for appropriate birth control methods. leukemia (CML) or Philadelphia chro-
Female pts must use contraception during mosome (Ph+) acute lymphoblastic
treatment and for at least 1 mo after treat- leukemia (ALL) for whom no other ki-
ment. Immediately report suspected preg- nase inhibitor therapy is indicated. Treat-
nancy. Male pts must use condoms with ment of adults with T315I-positive CML
spermicide during sexual activity, despite (chronic, accelerated, or blast phase) or
history of vasectomy. • Do not donate T315I-positive ALL (Ph+ ALL). Not indi-
blood. • Swallow capsules whole; do not cated for treatment of newly diagnosed
break, crush, or open. • Go from lying to chronic phase CML.
standing slowly (prevents postural hypoten-
sion, dizziness). Avoid tasks that require PRECAUTIONS
alertness, motor skills until response Contraindications: Hypersensitivity to
to drug is established. • Do not ponatinib. Cautions: Baseline hemato-
smoke. • Do not eat 2 hrs before or 2 hrs logic cytopenias; conditions predispos-
after dose. • Avoid alcohol. • Report ing to infection (e.g., diabetes, immu-
difficulty breathing, chest pain, extremity nocompromised pts, open wounds),
pain or swelling, dizziness, confusion. history of arterial/venous thrombosis
(e.g., CVA, DVT, MI, PE), cardiac dis-
ease, cardiac conduction disorders,
HF, hypertension; diabetes, electrolyte
imbalance, glaucoma, hepatic impair-
ponatinib ment, hyperlipidemia, GI perforation,
neuropathy (peripheral or cranial),
poe-na-ti-nib ocular disorders, pancreatitis or alco-
P (Iclusig) hol abuse, history of ischemia, vascular
j BLACK BOX ALERT jArterial stenosis; pts with high tumor burden;
occlusions have occurred, includ-
ing CVA, fatal MI, large arterial pts at risk for hemorrhage (e.g., his-
vessel stenosis of the brain, severe tory of intracranial/GI bleeding, co-
peripheral vascular disease agulation disorders, recent trauma;
requiring revascularization. Events concomitant use of anticoagulants,
may occur in pts with or without antiplatelets, NSAIDs).
cardiovascular risks, including
pts younger than 50 yrs of age. Ve- ACTION
nous thromboembolism, serious HF,
or left ventricular dysfunction were Inhibits viability of cells expressing na-
reported. Hepatotoxicity, including tive or mutant BCR-ABL tyrosine kinase,
fatal hepatic failure, may occur. including T315I mutation, created by the
Do not confuse ponatinib with Philadelphia chromosome abnormality.
afatinib, alectinib, dasatinib, Therapeutic Effect: Inhibits tumor cell
bosutinib, gefitinib, imatinib, growth and metastasis.
lapatinib, lenvatinib, neratinib,
or tofacitinib. PHARMACOKINETICS
uCLASSIFICATION
Widely distributed. Metabolized in
liver. Protein binding: greater than
PHARMACOTHERAPEUTIC: BCR-ABL 99%. Peak plasma concentration: 6
tyrosine kinase inhibitor. CLINI- hrs or less. Excreted in feces (87%),
CAL: Antineoplastic. urine (5%). Half-life: 24 hrs (Range:
12–66 hrs).

underlined – top prescribed drug


ponatinib 949

LIFESPAN CONSIDERATIONS with chronic or accelerated phase CML


Pregnancy/Lactation: Avoid preg- who have achieved a major cytogenetic
nancy; may cause fetal harm/malforma- response. If an adequate response has
tions. Unknown if distributed in breast been not achieved within 90 days, con-
milk. Breastfeeding not recommended sider discontinuation.
during treatment and for at least 6 days Dose Modification
after discontinuation. Females of repro- Hepatotoxicity
ductive potential and males with female CTCAE Grade 2 or greater serum ALT/
partners of reproductive potential should AST elevation (greater than 3 times
use effective contraception during treat- upper limit normal [ULN]): Withhold
ment and for at least 3 wks after discon- treatment until improved to Grade 1 or 0,
tinuation. May impair fertility in females. then resume dose based on occurrence.
Children: Safety and efficacy not estab- Occurrence at 45-mg dose: Resume
lished. Elderly: May have increased treatment at 30-mg dose. Occurrence
risk of adverse reactions/toxic effects. at 30-mg dose: Resume treatment at
Use caution. 15-mg dose. Occurrence at 15-mg
dose: Permanently discontinue. Serum
INTERACTIONS ALT/AST elevation greater than
DRUG: Strong CYP3A4 inhibitors or equal to 3 times ULN with con-
(e.g., clarithromycin, ketoconazole, current serum bilirubin elevation
ritonavir) may increase concentra- greater than 2 times ULN and se-
tion/effect. Strong CYP3A4 inducers rum alkaline phosphatase less than
(e.g., carBAMazepine, phenytoin, 2 times ULN: Permanently discontinue.
rifAMPin) may decrease concentration/
effect. May decrease therapeutic effect Neutropenia/Thrombocytopenia
of BCG (intravesical). HERBAL: St. ANC less than 1000 cells/mm3; plate-
John’s wort may decrease concentra- lets less than 50,000 cells/mm3: With-
tion/effect. FOOD: Grapefruit products hold treatment until ANC greater than or P
may increase concentration/effect. LAB equal to 1500 cells/mm3; or platelets greater
VALUES: May increase serum alkaline than or equal to 75,000 cells/mm3, then
phosphatase, amylase, ALT, AST, biliru- resume dose based on occurrence. First
bin, creatinine, lipase, triglycerides, uric occurrence: Resume treatment at 45-
acid. May decrease Hgb, Hct, leukocytes, mg dose. Second occurrence: Resume
lymphocytes, neutrophils, platelets; se- treatment at 30-mg dose. Third occur-
rum albumin, bicarbonate, phosphate. rence: Resume treatment at 15-mg dose.
May increase or decrease serum calcium,
Pancreatitis/Elevated Lipase
glucose, potassium, sodium.
Asymptomatic CTCAE Grade 1 or
AVAILABILITY (Rx) 2 serum lipase elevation: Consider
Tablets: 15 mg, 45 mg. withholding treatment or reducing dose.
Asymptomatic CTCAE Grade 3 or
ADMINISTRATION/HANDLING 4 serum lipase elevation (greater
than 2 times ULN); asymptomatic
PO
radiologic pancreatitis (Grade 2
• Give with or without food. • Admin-
pancreatitis): Withhold treatment
ister tablets whole; do not break, cut,
crush, or divide. until improved to Grade 1 or 0, then
resume dose based on occurrence.
INDICATIONS/ROUTES/DOSAGE Occurrence at 45-mg dose: Re-
CML, Ph+ ALL sume treatment at 30-mg dose. Occur-
PO: ADULTS, ELDERLY: 45 mg once rence at 30-mg dose: Resume treat-
daily. Consider dose reduction in pts ment at 15-mg dose. Occurrence at

Canadian trade name Non-Crushable Drug High Alert drug


950 ponatinib
15-mg dose: Permanently discontinue. requiring revascularization reported in
Grade 4 pancreatitis: Permanently dis- 35% of pts; may occur within 2 wks of
continue. initiation (even at reduced doses of 15
mg/day). Coronary artery occlusion, MI
Concomitant Use of Strong Cyp3a4 occurred in 21% of pts. Venous throm-
Inhibitors boembolism (DVT, PE, superficial throm-
Reduce initial dose to 30 mg. bophlebitis) occurred in 5–9% of pts.
Dosage in Renal Impairment
Life-threatening events including cardiac
Not specified; use caution. bradyarrhythmias (requiring pacemaker
implantation), complete heart block, sick
Dosage in Hepatic Impairment sinus syndrome, atrial fibrillation with
Mild, moderate, severe impairment bradycardic pauses, atrial fibrillation,
(Child-Pugh A, B, or C): Reduce initial SVT, ventricular tachycardia; emergent
dose to 30 mg. hypertension (68% of pts), GI/intracra-
nial hemorrhage (28% of pts), hepato-
SIDE EFFECTS toxicity (54% of pts), pancreatitis (6%),
Note: Percentages of side effects of HF, left ventricular dysfunction (6% of
chronic phase, accelerated phase, blast pts); infections including cellulitis, na-
phase CML; Ph+ ALL may vary. sopharyngitis, pneumonia, sepsis, upper
Frequent (69%–18%): Hypertension, ab- respiratory tract infection, UTI; ocular
dominal pain, fatigue, asthenia, head- toxicities including blindness, conjunc-
ache, dry skin, constipation, arthralgia, tival hemorrhage, cataracts, periorbital
nausea, pyrexia, burning sensation, edema, ocular hyperemia, iritis, irido-
hyperesthesia, hypoesthesia, neuralgia, cyclitis, ulcerative keratinitis; peripheral
paresthesia, dysgeusia, muscular weak- edema (31% of pts), pleural effusion (2%
ness, gait disturbance, areflexia, hypo- of pts), pericardial effusion (1% of pts);
tonia, restless legs syndrome, myalgia, peripheral neuropathy, polyneuropathy,
P extremity pain, back pain, diarrhea, vom- nerve compression (20% of pts) may oc-
iting. Occasional (17%–2%): Dyspnea, cur. Tumor lysis syndrome may present as
dizziness, peripheral edema, cough, bone acute renal failure, hypocalcemia, hyper-
pain, musculoskeletal pain, mucositis, uricemia, hyperphosphatemia. Revers-
aphthous stomatitis, lip blister, mouth ible posterior leukoencephalopathy may
ulceration, mucosal eruption, oral pain, include aphasia, cognition impairment,
oropharyngeal pain, stomatitis, tongue paralysis, vision loss, weakness. Pts with
ulceration, muscle spasm, conjunctival newly diagnosed CML have an increased
irritation, corneal abrasion/erosion, dry risk of severe toxicities. Improper wound
eye, hyperemia, eye pain, pruritus, de- healing, GI perforation may occur.
creased appetite, insomnia, decreased
weight, generalized pain, erythema, alo- NURSING CONSIDERATIONS
pecia, chills, blurry vision, tachycardia. BASELINE ASSESSMENT
ADVERSE EFFECTS/TOXIC Obtain CBC, BMP, LFT, serum ionized
REACTIONS calcium, phosphate, uric acid; vital signs;
Anemia, leukopenia, lymphopenia, neu- weight. Obtain pregnancy test in females of
tropenia, thrombocytopenia are expected reproductive potential. Question plans of
responses to therapy, but more severe re- breastfeeding. Receive full medication his-
actions including bone marrow failure, fe- tory including herbal products and screen
brile neutropenia may be life-­threatening. for interactions. Question history as listed
Fatal arterial occlusions including CVA, in Precautions. Screen for active infec-
MI, stenosis of large arterial vessel of the tion. Conduct ophthalmologic, neurologic
brain, severe peripheral ­vascular ­disease exam. Due to increased risk of tumor lysis

underlined – top prescribed drug


posaconazole 951
syndrome, assess adequate hydration prior bruising; persistent, severe abdominal
to initiation. Consider correcting elec- pain that radiates to the back [with or
trolyte abnormalities prior to initiation. without vomiting]); eye problems (blind-
Obtain dietary consult. Screen for risk of ness, blurred vision, eye inflammation or
bleeding; active infection. Assess skin for bleeding, severe eye or head pain); heart
rash, lesions. Offer emotional support. arrhythmias (chest pain, dizziness, faint-
ing, palpitations, slow or rapid heart rate,
INTERVENTION/EVALUATION
irregular heart rate); intestinal perfora-
Obtain ANC, CBC for myelosuppression tion (severe abdominal pain, fever, nau-
q2wks for 3 mos, then monthly thereaf- sea). • Treatment may depress your
ter. Monitor serum lipase monthly; BMP, immune system response and reduce your
LFT, serum ionized calcium, phosphate, ability to fight infection. Report symptoms
uric acid as indicated. Monitor ECG for of infection such as body aches, chills,
cardiac arrhythmias. Due to extremely cough, fatigue, fever. Avoid those with ac-
high risk for arterial occlusions, be vigi- tive infection. • Treatment may cause
lant when screening for CVA (aphasia, severe bone marrow depression; report
confusion, paresthesia, hemiparesis, sei- bruising, fatigue, fever, shortness of
zures), MI (chest pain, diaphoresis, left breath, weight loss, bleeding easily, bloody
arm/jaw pain, increased serum troponin, urine or stool. • Avoid pregnancy; may
ST segment elevation), vascular compro- cause birth defects or miscarriage. Fe-
mise. Be alert for serious infection, op- males and males of childbearing potential
portunistic infection, sepsis. Monitor for should use effective contraception during
GI perforation, hepatotoxicity, ocular dis- treatment and for at least 3 wks after final
ease, pancreatitis; symptoms of thrombo- dose. • Do not breastfeed during treat-
embolism (arm/leg pain, swelling; chest ment and for at least 6 days after final
pain, dyspnea, hypoxia, tachycardia), re- dose. • Report planned surgical/dental
versible posterior leukoencephalopathy, procedures. • Immediately report
tumor lysis syndrome; other toxicities as bleeding of any kind. • Do not ingest P
listed in Adverse Reactions/Toxic Effects. grapefruit products, herbal supple-
Monitor daily pattern of bowel activity, ments. • Do not take newly prescribed
stool consistency. Ensure adequate hy- medications unless approved by the pre-
dration, nutrition. Monitor weight, I&O. scriber who originally started treatment.
PATIENT/FAMILY TEACHING
• Treatment may cause life-threatening
arterial blood clots; report symptoms of
heart attack (chest pain, difficulty breath-
posaconazole
ing, jaw pain, nausea, pain that radiates to poe-sa-kon-a-zole
the left arm, sweating), stroke (blindness, (Noxafil, Posanol )
confusion, one-sided weakness, loss of Do not confuse Noxafil with
consciousness, trouble speaking, sei- minoxidil.
zures). • Report symptoms of DVT
(swelling, pain, hot feeling in the arms or uCLASSIFICATION
legs), lung embolism (difficulty breathing, PHARMACOTHERAPEUTIC: Azole de-
chest pain, rapid heart rate); liver prob- rivative. CLINICAL: Antifungal.
lems (abdominal pain, bruising, clay-col-
ored stool, amber or dark-colored urine,
yellowing of the skin or eyes); HF (diffi- USES
culty breathing, extremity swelling, sud- Prophylaxis of invasive Aspergillus and
den loss of breath, palpitations); inflam- Candida infections in pts 13 yrs and
mation of the pancreas (abdominal older (IV for pts 18 yrs and older) who

Canadian trade name Non-Crushable Drug High Alert drug


952 posaconazole
are at high risk for developing these in- decrease therapeutic effect of Saccha-
fections due to severely immunocompro- romyces boulardii. HERBAL: None
mised conditions. Treatment of oropha- significant. FOOD: Concentration higher
ryngeal candidiasis. OFF-LABEL: Salvage when given with food or nutritional
therapy of refractory invasive fungal supplements. Grapefruit products
infections, mucormycosis, pulmonary may decrease concentration/effects. LAB
infections. VALUES: May decrease WBC, RBC, Hgb,
Hct, platelets, serum calcium, potassium,
PRECAUTIONS magnesium. May increase serum glucose,
Contraindications: Hypersensitivity to bilirubin, ALT, AST, alkaline phosphatase.
posaconazole, other azole antifungals.
Coadministration with pimozide, quiNI- AVAILABILITY (Rx)
Dine (may cause QT prolongation, tor- Injection Solution: 300 mg/16.7 mL (18
sades de pointes), HMG-CoA reductase mg/mL). Oral Suspension: 40 mg/mL.
inhibitors metabolized by CYP3A4 (e.g., Tablets, Delayed-Release: 100 mg.
atorvastatin, lovastatin, simvastatin), si-
rolimus, ergot alkaloids. Cautions: Re- ADMINISTRATION/HANDLING
nal/hepatic impairment, hypokalemia,
IV
hypomagnesemia, pts at increased risk of
arrhythmias. Concomitant administration Reconstitution • Transfer 300 mg
of medications that prolong QT interval, (16.7 mL) posaconazole into 150 mL
pts with long QT syndrome. D5W or 0.9% NaCl bag.
Rate of administration • Infuse over
ACTION 90 min via central venous line. Must be
Inhibits synthesis of ergosterol, a vital infused through in-line filter (0.22 mi-
component of fungal cell wall formation. crons) or PVD filter.
Therapeutic Effect: Damages fungal Storage • Refrigerate vials. Once di-
P cell wall membrane, altering its function. luted, use immediately. May refrigerate
solution up to 24 hrs if not used immedi-
PHARMACOKINETICS ately.
Moderately absorbed following PO ad-
ministration. Absorption increased if PO
drug is taken with food. Widely distrib- • Administer with or within 20 min of
uted. Protein binding: 98%. Not signifi- full meal, liquid nutritional supplement,
cantly metabolized. Primarily excreted in or acidic carbonated beverage (e.g., gin-
feces. Half-life: 20–66 hrs. ger ale) (enhances absorption). • Store
oral suspension at room temperature.
LIFESPAN CONSIDERATIONS • Shake suspension well before use.
Pregnancy/Lactation: May cause • Tablets: Swallow whole; do not
fetal harm. Breastfeeding not recom- crush, cut, dissolve, or divide. Administer
mended. Children: Safety and efficacy with food.
not established in pts younger than 13
yrs. Elderly: No age-related precautions INDICATIONS/ROUTES/DOSAGE
noted. Note: The delayed-release tablets and
oral suspension are not to be used inter-
INTERACTIONS changeably.
DRUG: May increase concentration/ef-
fect of atorvastatin, cycloSPORINE, Prophylaxis of Invasive Aspergillus and
ergot alkaloids, phenytoin, rifabu- Candida
tin, simvastatin, sirolimus, tacroli- PO: ADULTS, ELDERLY, CHILDREN 13 YRS
mus, vinBLAStine, vinCRIStine. May AND OLDER: (Oral Suspension): 200

underlined – top prescribed drug


potassium ­acetate 953
mg (5 mL) 3 times/day, given with full NURSING CONSIDERATIONS
meal or liquid nutritional supplement.
(Delayed-Release): 300 mg twice daily BASELINE ASSESSMENT
on first day, then 300 mg once daily. Obtain BMP, LFT, ECG. Receive full medi-
IV: 300 mg twice daily on first day, then cation history and screen for interactions
300 mg once daily thereafter. (esp. drugs known to prolong QT interval).
Oropharyngeal Candidiasis INTERVENTION/EVALUATION
PO: ADULTS, ELDERLY, CHILDREN 13 YRS Monitor LFT periodically. Monitor daily
AND OLDER: 100 mg twice daily for 1 day, pattern of bowel activity, stool consis-
then 100 mg once daily for 13 days. tency. Obtain order for antiemetic if
excessive vomiting occurs. Monitor B/P
Oropharyngeal Candidiasis Refractory to for hypertension, hypotension. Assess for
Fluconazole lower extremity edema.
PO: ADULTS, ELDERLY: (Suspension):
400 mg twice daily for 3 days, then 400 PATIENT/FAMILY TEACHING
mg once daily for up to 28 days. HIV- • Take each dose with full meal or liquid
INFECTED PTS: (Suspension): 400 mg nutritional supplement. • Report severe
twice daily on day 1, then 400 mg once diarrhea, vomiting, chest pain, yellowing of
daily for 7–14 days (28 days in azole re- skin/eyes. • Maintain strict oral hygiene.
fractory pts).
Dosage in Renal Impairment
PO: No dose adjustment. IV: Avoid use
in pts with CrCl less than 50 mL/min. potassium
Dosage in Hepatic Impairment ­acetate
No dose adjustment.
potassium P
SIDE EFFECTS
Common (42%–24%): Diarrhea, nausea, ­bicarbonate/citrate
vomiting, headache, abdominal pain,
cough. Frequent (20%–15%): Constipa- (Effer-K, Klor-Con EF)
tion, rigors, rash, hypertension, fatigue,
insomnia, mucositis, musculoskel- potassium chloride
etal pain, edema of lower extremities,
herpes simplex, anorexia. Occasional (Kaon-Cl, Klor-Con, Klor-Con M10,
(14%–8%): Hypotension, epistaxis, Klor-Con M20, Micro-K)
tachycardia, pharyngitis, dizziness, pru- Do not confuse Micro-K with
ritus, arthralgia, dyspepsia, back pain, Macrobid or Micronase.
generalized edema, weakness.
uCLASSIFICATION
ADVERSE EFFECTS/TOXIC PHARMACOTHERAPEUTIC: Electro-
REACTIONS lyte. CLINICAL: Potassium replen-
Bacteremia occurs in 18% of pts; up- isher.
per respiratory tract infection occurs in
7%. Allergic/hypersensitivity reactions,
QT prolongation, hemolytic uremic syn- USES
drome, thrombotic thrombocytopenic Potassium acetate, potassium bi-
purpura, pulmonary embolus have been carbonate/citrate: Treatment, preven-
reported.

Canadian trade name Non-Crushable Drug High Alert drug


954 potassium ­acetate
tion of hypokalemia when necessary to nificant. FOOD: None known. LAB VAL-
avoid chloride or acid/base imbalance UES: None known.
(requires bicarbonate). Potassium
chloride: Treatment, prevention of hy- AVAILABILITY (Rx)
pokalemia. Potassium Acetate
Injection Solution: 2 mEq/mL.
PRECAUTIONS Potassium Bicarbonate And
Contraindications: Acetate: Severe re- Potassium Citrate
nal impairment, adrenal insufficiency, Tablets for Solution: (Effer-K): 10 mEq,
hyperkalemia. Chloride: Renal failure, 20 mEq, 25 mEq. (Klor-Con EF): 25 mEq.
hyperkalemia, conditions in which po- Potassium Chloride
tassium retention is present. Solid oral Injection Solution: 2 mEq/mL. Oral
dosage form in pts in whom there is Solution: 20 mEq/15 mL, 40 mEq/15
structural, pathologic cause for delay in mL. Powder for Oral Solution: 20 mEq/
passage through GI tract. Cautions: Car- packet, 25 mEq/packet.
diac disease, acid-base disorders, po- Capsules, Extended-Release: (Micro-K): 8
tassium-altering disorders, digitalized mEq, 10 mEq. Tablets, Extended-Re-
pts, concomitant therapy that increases lease: 8 mEq, 10 mEq, 15 mEq, 20 mEq.
serum potassium (e.g., ACE inhibitors),
renal impairment. Do not administer IV ADMINISTRATION/HANDLING
undiluted.
IV
ACTION Reconstitution • For IV infusion only,
Necessary for multiple cellular metabolic must dilute before administration, mix
processes. Primary action is intracellular. well, infuse slowly. • Avoid adding po-
Therapeutic Effect: Required for nerve tassium to hanging IV.
impulse conduction, contraction of car- Rate of administration • Routinely,
P diac, skeletal, smooth muscle; maintains give at concentration of no more than 40
normal renal function, acid-base balance. mEq/L, no faster than 10 mEq/hr for pe-
ripheral infusion, 20–40 mEq/hr for cen-
PHARMACOKINETICS tral infusion.
Well absorbed from GI tract. Enters cells Storage • Store at room temperature.
by active transport from extracellular Use admixtures within 24 hrs.
fluid. Primarily excreted in urine.
PO
LIFESPAN CONSIDERATIONS • Take with or after meals, with full glass
Pregnancy/Lactation: Unknown if of water (decreases GI upset). • Liq-
drug crosses placenta or is distributed in uids, powder, effervescent tablets: Mix,
breast milk. Children: No age-related dissolve with juice, water before adminis-
precautions noted. Elderly: May be at in- tering. • Do not break, crush, dissolve,
creased risk for hyperkalemia. Age-related or divide tablets; give whole.
ability to excrete potassium is reduced.
IV INCOMPATIBILITIES
INTERACTIONS Amphotericin B complex (Abelcet,
DRUG: ACE inhibitors (e.g., enala- AmBisome, Amphotec), phenytoin (Di-
pril, lisinopril), eplerenone, po- lantin).
tassium-containing medications,
potassium-sparing diuretics (e.g., IV COMPATIBILITIES
spironolactone, triamterene), salt Amiodarone (Cordarone), atropine, az-
substitutes may increase serum potas- treonam (Azactam), calcium gluconate,
sium concentration. HERBAL: None sig- cefepime (Maxipime), ciprofloxacin
underlined – top prescribed drug
potassium ­acetate 955
(Cipro), clindamycin (Cleocin), dexa- Dosage in Renal/Hepatic Impairment
methasone (Decadron), dexmedetomi- No dose adjustment. Use caution with
dine (Precedex), digoxin (Lanoxin), dil- potassium acetate (may increase serum
TIAZem (Cardizem), diphenhydrAMINE aluminum and/or potassium).
(Benadryl), DOBUTamine (Dobutrex),
DOPamine (Intropin), enalapril (Vaso- SIDE EFFECTS
tec), famotidine (Pepcid), fluconazole Occasional: Nausea, vomiting, diarrhea,
(Diflucan), furosemide (Lasix), granis- flatulence, abdominal discomfort with
etron (Kytril), heparin, hydrocortisone distention, phlebitis with IV administra-
(Solu-CORTEF), insulin, lidocaine, LO- tion (particularly when potassium con-
Razepam (Ativan), magnesium sulfate, centration of greater than 40 mEq/L is
methylPREDNISolone (SOLU-Medrol), infused). Rare: Rash.
metoclopramide (Reglan), midazolam
(Versed), milrinone (Primacor), mor- ADVERSE EFFECTS/TOXIC
phine, norepinephrine (Levophed), on- REACTIONS
dansetron (Zofran), oxytocin (Pitocin), Hyperkalemia (more common in elderly,
piperacillin and tazobactam (Zosyn), pts with renal impairment) manifested as
procainamide (Pronestyl), propofol (Di- paresthesia, motor weakness, cold skin,
privan), propranolol (Inderal). hypotension, confusion, irritability, pa-
ralysis, cardiac arrhythmias. Too-rapid
INDICATIONS/ROUTES/DOSAGE infusion may cause cardiac arrhythmia,
Treatment of Hypokalemia ventricular fibrillation, cardiac arrest.
Potassium Acetate
IV: ADULTS, ELDERLY: 5–10mEq/dose NURSING CONSIDERATIONS
(Maximum: 40 mEq/dose) to infuse BASELINE ASSESSMENT
over 2–3 hrs. Usual Range: 40–100 Assess for hypokalemia (weakness, fa-
mEq/day. tigue, polyuria, polydipsia). PO should
Dose/Rate Guidelines P
be given with food or after meals with full
Greater glass of water, fruit juice (minimizes GI
than 2.5– 2.5 mEq/L irritation).
Serum potassium 3.5 mEq/L or less
INTERVENTION/EVALUATION
Maximum infusion 10 mEq/ 40 mEq/hr
rate hr Monitor serum potassium, calcium,
Maximum 24-hr 200 mEq 400 mEq phosphate. If GI disturbance is noted,
dose dilute preparation further or give with
meals. Be alert to decreased urinary out-
Potassium Chloride put (may be indication of renal insuffi-
PO: ADULTS, ELDERLY: Mild to moder- ciency). Check IV site closely during infu-
ate: Initially, 10–20 mEq given 2–4 sion for evidence of phlebitis (heat, pain,
times/day. Severe: Initially, 40 mEq red streaking of skin over vein, hardening
given 3–4 times/day. (May also give 20 of vein), extravasation (swelling, pain).
mEq q2–3h in conjunction with careful Be alert to evidence of hyperkalemia
monitoring.) CHILDREN: Initially, 1–2 (skin pallor/coldness, paresthesia, feel-
mEq/kg, then as needed based on lab ing of heaviness of lower extremities).
values.
IV: ADULTS, ELDERLY: 10 mEq/hr (or PATIENT/FAMILY TEACHING
less); repeat as needed based on lab • Foods rich in potassium include beef,
values. CHILDREN: 0.5–1 mEq/kg/dose veal, ham, chicken, turkey, fish, milk,
(Maximum: 40 mEq); repeat as needed bananas, dates, prunes, raisins, avoca-
based on lab values. dos, watermelon, cantaloupe, apricots,
molasses, beans, yams, broccoli, brus-

Canadian trade name Non-Crushable Drug High Alert drug


956 PRALAtrexate
sels sprouts, lentils, potatoes, spin- INTERACTIONS
ach. • Report numbness, feeling of DRUG: NSAIDs (e.g., ibuprofen, ke-
heaviness of lower extremities, weak- torolac, naproxen), probenecid,
ness, unusual fatigue. salicylates (e.g., aspirin), trime-
thoprim/sulfamethoxazole may delay
clearance, increase concentration. May
decrease the therapeutic effect; increase
PRALAtrexate adverse effects of vaccines (live).
HERBAL: Echinacea may decrease con-
pral-a-trex-ate centration/effects. FOOD: None known.
(Folotyn) LAB VALUES: May decrease RBC, WBC,
Do not confuse Folotyn with Hgb, Hct, platelet count, serum potas-
Focalin, or PRALAtrexate with sium. May increase serum ALT, AST.
methotrexate or PEMEtrexed.
uCLASSIFICATION AVAILABILITY (Rx)
PHARMACOTHERAPEUTIC: Antime- Injection Solution: 20 mg/mL.
tabolite. CLINICAL: Antineoplastic.
ADMINISTRATION/HANDLING
b ALERT c May be carcinogenic, muta-
USES genic, teratogenic. Handle with extreme
Treatment of relapsed or refractory pe- care during preparation/administration.
ripheral T-cell lymphoma (PTCL). OFF- Wear gloves when preparing solution. If
LABEL: Treatment of relapsed/refractory powder or solution comes in contact
cutaneous T-cell lymphoma. with skin, wash immediately, thoroughly
with soap, water.
PRECAUTIONS
IV
P Contraindications: Hypersensitivity to
PRALAtrexate. Cautions: Moderate to Reconstitution • Withdraw calcu-
severe renal impairment, hepatic im- lated dose into syringe for immediate
pairment. Avoid use in end-stage renal use. • Intended for single use
disease. only. • Do not dilute.
Rate of administration • Administer
ACTION as IV push over 3–5 min into IV infusion
Folate analogue metabolic inhibitor of 0.9% NaCl.
that competes with enzymes neces- Storage • Refrigerate vials until use,
sary for tumor cell reproduction. protect from light. Stable at room tem-
Inhibits DNA, RNA, protein synthesis. perature for 72 hrs. • Discard vial if
Therapeutic Effect: Inhibits tumor solution is discolored (solution should
growth. appear clear to yellow) or particulate
matter is present.
PHARMACOKINETICS
Protein binding: 67%. Partially excreted IV INCOMPATIBILITIES
in urine. Half-life: 12–18 hrs. Do not mix with any other medication.
LIFESPAN CONSIDERATIONS INDICATIONS/ROUTES/DOSAGE
Pregnancy/Lactation: May cause fetal b ALERT c Prior to any dose, mucositis
harm. Unknown if drug is distributed in should be no higher than CTCAE Grade 1,
breast milk. Children: Safety and ef- platelets 100,000 cells/mm3 or greater for
ficacy not established. Elderly: No age- first dose and 50,000 cells/mm3 or greater
related precautions noted. for subsequent doses, and absolute neutro-
underlined – top prescribed drug
pramipexole 957
phil count (ANC) 1,000 cells/mm3 or NURSING CONSIDERATIONS
greater. Pt should begin taking oral folic
acid (1 mg) daily starting 10 days prior to BASELINE ASSESSMENT
first IV PRALAtrexate dose and continue for Evaluate baseline CBC with differential,
30 days after last dose. Pt should also re- renal function, LFT, serum potassium
ceive vitamin B12 (1 mg) IM injection no level. Question for possibility of preg-
more than 10 wks prior to first IV PRALA- nancy before initiating therapy. Assess
trexate dose and every 8–10 wks thereafter. baseline vital signs, temperature. Anti-
emetics before and during therapy may
Refractory/Relapsed Peripheral T-Cell alleviate nausea/vomiting. Initiate folic
Lymphoma acid, vitamin B12 administration prior to
IV: ADULTS, ELDERLY: 30 mg/m2 ad- and throughout therapy.
ministered once wkly for 6 wks in 7-wk
cycles. Dose may be decreased to 20 mg/ INTERVENTION/EVALUATION
m2 to manage adverse reactions. Con- Prior to any dose: mucositis should be
tinue until disease progression or unac- Grade 1 or less. Platelet count 100,000
ceptable toxicity. cells/mm3 or greater for first dose
(50,000 cells/mm3 or greater for all
Dosage in Renal Impairment subsequent doses). Absolute neutrophil
Monitor for toxicities. Avoid use in end- count (ANC) 1,000 cells/mm3 or greater.
stage renal disease. Assess for signs of mucositis (oropha-
Dosage in Hepatic Impairment
ryngeal ulcers, oral/throat pain, local
CTCAE Grade 3: Withhold dose; de- infection). Monitor for signs of hemato-
crease to 20 mg/m2 when Grade 2 or less. logic toxicity, sepsis (fever, signs of local
CTCAE Grade 4: Discontinue.
infection, altered CBC results). Monitor
hepatic/renal function. Monitor for hypo-
SIDE EFFECTS kalemia (muscle cramps, weakness, ECG
Common (70%–36%): Mucositis, nausea,
changes). P
fatigue. Frequent (34%–10%): Constipa- PATIENT/FAMILY TEACHING
tion/diarrhea, pyrexia, edema, cough, • Explain importance of folic acid, vita-
epistaxis, vomiting, dyspnea, anorexia, min B12 therapy to reduce adverse ef-
rash, throat/abdominal/back pain, night fects. • Maintain strict oral hy-
sweats, asthenia, tachycardia, upper re- giene. • Do not have immunizations
spiratory infection. without physician’s approval (drug low-
ADVERSE EFFECTS/TOXIC ers body’s resistance). • Avoid crowds,
REACTIONS those with infection. • Promptly report
fever, sore throat, signs of local infection,
Hematologic toxicity, resulting from unusual bruising/bleeding from any site.
blood dyscrasias, may manifest as throm- • Use nonhormonal contraception.
bocytopenia (41% of pts), anemia (34% • Report persistent nausea/vomiting.
of pts), neutropenia (24% of pts), leu-
kopenia (11% of pts). High potential for
development of mucositis (70% of pts).
Mucositis is less severe when folic acid,
vitamin B12 therapy is ongoing. Sepsis,
pyrexia, febrile neutropenia, dehydration
pramipexole
have occurred. Overdosage requires gen- pram-i-pex-ole
eral supportive care. Prompt administra- (Apo-Pramipexole , Mirapex,
tion of leucovorin should be considered Mirapex ER)
in case of overdose, based on mechanism
of action of PRALAtrexate.
Canadian trade name Non-Crushable Drug High Alert drug
958 pramipexole
Do not confuse Mirapex with INTERACTIONS
Mifeprex or MiraLax. DRUG: Antipsychotic agents (e.g.,
uCLASSIFICATION
haloperidol) may decrease therapeutic
effect. Levodopa-containing ­products
PHARMACOTHERAPEUTIC: DO- may increase the hypotensive effect.
Pamine receptor agonist. CLINI- HERBAL: Herbals with hypotensive
CAL: Antiparkinson agent. properties (e.g., garlic, ginger, gingko
biloba) may increase hypotensive effect.
FOOD: All foods delay peak drug plasma
USES
levels by 1 hr (extent of absorption not af-
Mirapex: Treatment of Parkinson’s dis- fected). LAB VALUES: None significant.
ease, moderate to severe primary restless
legs syndrome. Mirapex ER: Treatment AVAILABILITY (Rx)
of Parkinson’s disease. OFF-LABEL: Im- Tablets:0.125 mg, 0.25 mg, 0.5 mg,
mediate-Release: Depression (due to 0.75 mg, 1 mg, 1.5 mg.
bipolar disorder), fibromyalgia.
Tablets, Extended-Release: (Mirapex
PRECAUTIONS ER): 0.375 mg, 0.75 mg, 1.5 mg, 2.25
mg, 3 mg, 3.75 mg, 4.5 mg.
Contraindications: Hypersensitivity to
pramipexole. Cautions: History of or- ADMINISTRATION/HANDLING
thostatic hypotension, pts at risk for PO
hypotension, syncope, hallucinations, Mirapex: • Give without regard to
renal impairment (extended-release food. Mirapex ER: • Give once daily,
not recommended with CrCl less than without regard to food. • Give whole; do
30 mL/min), concomitant use of CNS not break, crush, dissolve, or divide tablets.
depressants, preexisting dyskinesia, el-
derly pts. INDICATIONS/ROUTES/DOSAGE
P
Parkinson’s Disease
ACTION
Note: When discontinuing, reduce dose
Stimulates DOPamine receptors in stria- by 0.75 mg/day until daily dose is 0.75
tum and substantia nigra. Therapeutic mg once daily, then reduce by 0.375 mg/
Effect: Relieves signs/symptoms of Par- day thereafter.
kinson’s disease. Improves motor func- PO: (Immediate-Release): ADULTS,
tion. ELDERLY: Initially, 0.125 mg 3 times/day.
Increase no more frequently than every
PHARMACOKINETICS 5–7 days. Maintenance: 0.5–1.5 mg
Rapidly, extensively absorbed after PO 3 times/day. (Extended-Release): Ini-
administration. Protein binding: 15%. tially, 0.375 mg once daily. May increase
Widely distributed. Steady-state con- to 0.75 mg, then by 0.75-mg increments
centrations achieved within 2 days. Pri- no more frequently than 5–7 days. Max-
marily excreted in urine. Not removed imum: 4.5 mg once daily. Note: May
by hemodialysis. Half-life: 8 hrs (12 switch overnight from immediate-release
hrs in pts older than 65 yrs). to extended-release at same daily dose.

LIFESPAN CONSIDERATIONS Restless Legs Syndrome


Note: When discontinuing, gradually re-
Pregnancy/Lactation: Unknown if
duce dose q4–7 days.
drug is distributed in breast milk. Chil-
PO: ADULTS, ELDERLY: (Immediate-­
dren: Safety and efficacy not estab-
Release): Initially, 0.125 mg once daily
lished. Elderly: Increased risk of hal-
2–3 hrs before bedtime. May increase to
lucinations.

underlined – top prescribed drug


prasugrel 959
0.25 mg after 4–7 days, then to 0.5 mg syndrome: Frequent (16%): Headache,
after 4–7 days (interval is 14 days in pts nausea. Occasional (13%–9%): Insom-
with renal impairment). Maximum: 0.75 nia, fatigue. Rare (6%–3%): Drowsiness,
mg/day. constipation, diarrhea, dry mouth.
Dosage in Renal Impairment ADVERSE EFFECTS/TOXIC
Dosage and frequency are modified REACTIONS
based on creatinine clearance. Vascular disease, atrial fibrillation, arrhyth-
mias, pulmonary embolism, impulsive/
Parkinson’s Disease
compulsive behavior (pathological gam-
Immediate-Release
bling, hypersexuality, binge eating) have
Creatinine Initial Maximum been reported.
Clearance Dosage Dosage
30–50 mL/ 0.125 mg 0.75 mg 3 NURSING CONSIDERATIONS
min twice daily times/day
15–29 mL/ 0.125 mg once 1.5 mg once BASELINE ASSESSMENT
min daily daily Parkinson’s disease: Assess for
tremor, muscle weakness and rigidity,
Extended-Release
ataxia. Restless legs syndrome: Assess
CrCl 30–50 mL/min: Initially, 0.375 frequency of symptoms, sleep pattern.
mg every other day. May increase by
0.375 mg/day in 7 days or longer. Maxi- INTERVENTION/EVALUATION
mum: 2.25 mg once daily. CrCl less Assess for clinical improvement. Assist
than 30 mL/min: Not recommended. with ambulation if dizziness occurs. As-
sess for constipation; encourage fiber,
Restless Legs Syndrome
fluids, exercise.
No dose adjustment.
PATIENT/FAMILY TEACHING
Dosage in Hepatic Impairment P
• Inform pt that hallucinations may occur,
No dose adjustment. esp. in the elderly. • Go from lying to
SIDE EFFECTS standing slowly. • Avoid tasks that require
alertness, motor skills until response to
Frequent: Early Parkinson’s disease drug is established. • If nausea occurs,
(28%–10%): Nausea, asthenia, dizzi- take medication with food. • Avoid abrupt
ness, drowsiness, insomnia, constipa- withdrawal. • Avoid alcohol. • Report
tion. Advanced Parkinson’s disease new or increased impulsive/compulsive be-
(53%–17%): Orthostatic hypoten- haviors (e.g., gambling, sexual urges, com-
sion, extrapyramidal reactions, insom- pulsive eating or buying).
nia, dizziness, hallucinations. Occa-
sional: Early Parkinson’s disease
(5%–2%): Edema, malaise, confusion,
amnesia, akathisia, anorexia, dysphagia, prasugrel
peripheral edema, vision changes, impo-
tence. Advanced Parkinson’s disease pra-soo-grel
(10%–7%): Asthenia, drowsiness, con- (Effient)
fusion, constipation, abnormal gait, dry j BLACK BOX ALERT jSerious,
mouth. Rare: Advanced Parkinson’s sometimes fatal, hemorrhage may
disease (6%–2%): General edema, occur.
malaise, angina, amnesia, tremor, uri- Do not confuse Effient with
nary frequency/incontinence, dyspnea, Effexor, or prasugrel with
rhinitis, vision changes. Restless legs praziquantel.

Canadian trade name Non-Crushable Drug High Alert drug


960 prasugrel
uCLASSIFICATION INTERACTIONS
PHARMACOTHERAPEUTIC: Thieno- DRUG: Aspirin, NSAIDs (e.g., ibu-
pyridine derivative inhibitor. CLINI- profen, ketorolac, naproxen), war-
CAL: Antiplatelet agent. farin may increase risk of bleeding.
Apixaban, dabigatran, edoxaban, ri-
USES varoxaban may increase anticoagulant
Reduction of thrombotic cardiovascular effect. HERBAL: Herbals with anticoag-
events (MI, CVA, stent thrombosis) in pts ulant/antiplatelet properties (e.g.,
with acute coronary syndrome (unstable garlic, ginger, ginseng, ginkgo bi-
angina, non–ST-segment elevation MI, loba) may increase concentration/effect.
FOOD: None known. LAB VALUES: May
ST-segment MI) who are to be managed
with percutaneous coronary intervention decrease Hgb, Hct, WBC, platelet count.
(PCI). OFF-LABEL: Initial treatment of un- May increase bleeding time, serum cho-
stable angina, STEMI in pts undergoing lesterol, ALT, AST.
PCI with allergy or major GI intolerance AVAILABILITY (Rx)
to aspirin.
Tablets: 5 mg, 10 mg.
PRECAUTIONS
ADMINISTRATION/HANDLING
Contraindications: Hypersensitivity to
PO
prasugrel. Active bleeding, prior tran-
sient ischemic attack (TIA), CVA. Cau- • Give without regard to food. • Do
tions: Pts who undergo coronary artery
not crush tablet.
bypass graft (CABG) after receiving pra- INDICATIONS/ROUTES/DOSAGE
sugrel, pts at risk for bleeding (age 75
Acute Coronary Syndrome
yrs or older, body weight less than 60 kg,
b ALERT c Consider 5 mg once daily
recent trauma/surgery, recent GI bleed-
ing or active peptic ulcer disease, severe for pts weighing less than 60 kg. Not
P recommended in pts 75 yrs and older.
hepatic impairment).
PO: ADULTS, ELDERLY: Initially, 60-mg
ACTION loading dose, then 10 mg once daily (in
Inhibits binding of the enzyme adenosine combination with aspirin) for at least 12
phosphate (ADP) to its platelet receptor, mos.
which prevents activation of the GPIIb/ Dosage in Renal/Hepatic Impairment
IIIa receptor complex. Therapeutic Ef- No dose adjustment.
fect: Inhibits platelet aggregation.
SIDE EFFECTS
PHARMACOKINETICS
Occasional (8%–4%): Hypertension, mi-
Rapidly absorbed, with peak concentra- nor bleeding, headache, back pain, dys-
tion occurring 30 min following admin- pnea, nausea, dizziness. Rare (less than
istration. Metabolized in liver. Protein 4%): Cough, hypotension, fatigue, non-
binding: 98%. Excreted in urine (68%), cardiac chest pain, bradycardia, rash, py-
feces (27%). Half-life: 7 hrs. rexia, peripheral edema, extremity pain,
LIFESPAN CONSIDERATIONS diarrhea.
Pregnancy/Lactation: Unknown if ADVERSE EFFECTS/TOXIC
drug crosses placenta or is distributed in REACTIONS
breast milk. Children: Safety and efficacy Major bleeding (intracranial hemor-
not established. Elderly: May have in- rhage, epistaxis, GI bleeding, hemop-
creased risk for intracranial hemorrhage; tysis, SQ hematoma, postprocedural
caution advised in pts 75 yrs and older. hemorrhage, retroperitoneal hemor-
underlined – top prescribed drug
pravastatin 961
rhage, retinal hemorrhage) has been FIXED-COMBINATION(S)
reported. Severe thrombocytopenia, Pravigard: pravastatin/aspirin (anti-
anemia, abnormal hepatic function, coagulant): 20 mg/81 mg, 40 mg/81
anaphylactic reaction, angioedema, mg, 80 mg/81 mg, 20 mg/325 mg, 40
atrial fibrillation occur rarely. Over- mg/325 mg, 80 mg/325 mg.
dosage may require platelet transfusion
to restore clotting ability. uCLASSIFICATION
PHARMACOTHERAPEUTIC: Hydroxy-
NURSING CONSIDERATIONS
methylglutaryl CoA (HMG-CoA) re-
BASELINE ASSESSMENT ductase inhibitor. CLINICAL: Anti-
Obtain baseline vital signs, CBC, ECG, LFT. hyperlipidemic.
Question history of intracranial hemor-
rhage, GI bleeding, ulcers, recent surgery USES
or trauma. Adjunct to diet in the treatment of pri-
INTERVENTION/EVALUATION mary hyperlipidemias and mixed dyslip-
Monitor vital signs for changes in B/P, idemias to reduce total cholesterol, LDL
pulse. Assess for signs of unusual bleed- cholesterol, apolipoprotein B, triglycer-
ing or hemorrhage, pain. Monitor plate- ides; increase HDL cholesterol. Reduces
let count, LFT, ECG for changes from risk of MI, revascularization, and mortal-
baseline. ity in hypercholesterolemia without clini-
cally evident CHD. Reduces mortality risk
PATIENT/FAMILY TEACHING in pts with CHD. Reduces elevated triglyc-
• It may take longer to stop minor erides in hypertriglyceridemia. Treatment
bleeding during drug therapy. Report of heterozygous familial hypercholester-
unusual bleeding/bruising, blood olemia in pediatric pts 8–18 yrs.
noted in stool or urine, chest/back
pain, extremity pain, symptoms of PRECAUTIONS P
stroke. • Monitor for dys- Contraindications: Hypersensitivity to
pnea. • Report fever, weakness, ex- pravastatin. Active hepatic disease or
treme skin paleness, purple skin unexplained, persistent elevations of
patches, yellowing of skin or eyes, LFT results. Pregnancy, breastfeeding.
changes in mental status. • Do not Cautions: History of hepatic disease,
discontinue drug therapy without phy- substantial alcohol consumption. With-
sician approval. • Inform physicians, holding/discontinuing pravastatin may be
dentists before undergoing any invasive necessary when pt is at risk for renal fail-
procedure or surgery. ure secondary to rhabdomyolysis, elderly.
ACTION
Interferes with cholesterol biosynthesis
pravastatin by preventing conversion of HMG-CoA
reductase to mevalonate, a precursor to
pra-va-sta-tin cholesterol. Therapeutic Effect: Low-
(Pravachol) ers LDL, VLDL cholesterol, plasma tri-
Do not confuse pravastatin with glycerides; increases HDL.
atorvastatin, lovastatin, nystatin,
pitavastatin, or simvastatin, or PHARMACOKINETICS
Pravachol with Prevacid, Prini- Rapidly absorbed from GI tract. Pro-
vil, or propranolol. tein binding: 50%. Metabolized in liver.
Primarily excreted in feces via biliary

Canadian trade name Non-Crushable Drug High Alert drug


962 pravastatin
system. Not removed by hemodialysis. Dosage with Clarithromycin
Half-life: 2–3 hrs. (Half-life including Maximum: 40 mg/day.
all metabolites: 77 hrs.)
Dosage with CycloSPORINE
LIFESPAN CONSIDERATIONS Initially, 10 mg/day.
ADULTS, ELDERLY:
Pregnancy/Lactation: Contraindi- Maximum: 20 mg/day.
cated in pregnancy (suppression of Dosage in Renal Impairment
cholesterol biosynthesis may cause fe- For adults, give 10 mg/day initially. Titrate
tal toxicity) and lactation. Small amount to desired response.
is distributed in breast milk, but there
is risk of serious adverse reactions in Dosage in Hepatic Impairment
breastfeeding infants. Breastfeeding not See contraindications.
recommended. Children/Elderly: No
age-related precautions noted. SIDE EFFECTS
INTERACTIONS Pravastatin is generally well tolerated.
DRUG: CycloSPORINE, clarithro- Side effects are usually mild and tran-
mycin, colchicine, erythromycin, sient. Occasional (7%–4%): Nausea,
gemfibrozil, niacin increase risk of vomiting, diarrhea, constipation, ab-
myopathy, rhabdomyolysis. Bile acid dominal pain, headache, rhinitis, rash,
sequestrants (e.g., cholestyramine) pruritus. Rare (3%–2%): Heartburn,
may decrease absorption. HERBAL: None myalgia, dizziness, cough, fatigue, flu-
significant. FOOD: Red yeast rice con- like symptoms, depression, photosen-
tains 2.4 mg lovastatin per 600 mg rice sitivity.
(may increase adverse effects). LAB VAL-
UES: May increase serum creatine kinase ADVERSE EFFECTS/TOXIC
(CK), transaminase. REACTIONS
P Potential for malignancy, cataracts. Hy-
AVAILABILITY (Rx) persensitivity, myopathy occur rarely.
Tablets: 10 mg, 20 mg, 40 mg, 80 mg. Rhabdomyolysis has been reported.

ADMINISTRATION/HANDLING NURSING CONSIDERATIONS


PO BASELINE ASSESSMENT
• Give without regard to food. Obtain dietary history, esp. fat consump-
INDICATIONS/ROUTES/DOSAGE tion. Question for possibility of preg-
nancy before initiating therapy. Assess
b ALERT c Prior to initiating therapy, pt
baseline serum lab results (cholesterol,
should be on standard cholesterol-low- triglycerides, LFT).
ering diet for 3–6 mos. Low-cholesterol
diet should be continued throughout INTERVENTION/EVALUATION
pravastatin therapy. Monitor serum cholesterol, triglyceride
lab results for therapeutic response.
Hyperlipidemia, Prevention of Coronary/
Monitor LFT, CPK. Monitor daily pat-
Cardiovascular Events
tern of bowel activity, stool consistency.
PO: ADULTS, ELDERLY: Initially, 40 mg/
Assess for headache, dizziness (provide
day. Titrate to desired response. Range: assistance as needed). Assess for rash,
10–80 mg/day. pruritus. Be alert for malaise, muscle
Heterozygous Familial cramping/weakness; if accompanied by
Hypercholesterolemia fever, may require discontinuation of
PO: CHILDREN 14–18 YRS: 40 mg/day. medication.
CHILDREN 8–13 YRS: 20 mg/day.
underlined – top prescribed drug
prednisoLONE 963

PATIENT/FAMILY TEACHING tions, varicella, live or attenuated virus


• Follow special diet (important part vaccines. Cautions: Hyperthyroidism,
of treatment). • Periodic lab tests cirrhosis, ocular herpes simplex, respi-
are essential part of therapy. • Re- ratory tuberculosis, untreated systemic
port promptly any muscle pain/weak- infections, renal/hepatic impairment,
ness, esp. if accompanied by fever, diabetes, cataracts, glaucoma, seizure
malaise. • Avoid tasks that require disorder, peptic ulcer disease, osteopo-
alertness, motor skills until response rosis, myasthenia gravis, hypertension,
to drug is established (potential for HF, ulcerative colitis, thromboembolic
dizziness). • Use nonhormonal con- disorders, elderly pts.
traception. • Avoid direct exposure
to sunlight. ACTION
Inhibits accumulation of inflammatory
cells at inflammation sites, phagocyto-
sis, lysosomal enzyme release/synthesis,
prednisoLONE release of mediators of inflammation.
Therapeutic Effect: Prevents/sup-
pred-niss-oh-lone presses cell-mediated immune reactions.
(Millipred, Omnipred, Orapred Decreases/prevents tissue response to
ODT, Pred Forte, Pred Mild, inflammatory process.
Veripred)
Do not confuse Pediapred with PHARMACOKINETICS
Pediazole, prednisoLONE with Protein binding: 65%–91%. Metabolized
predniSONE or primidone, or in liver. Excreted in urine. Half-life: 3.6
Prelone with PROzac. hrs.
FIXED-COMBINATION(S) LIFESPAN CONSIDERATIONS
Blephamide: prednisoLONE/sulfacet- Pregnancy/Lactation: Crosses pla- P
amide (an anti-infective): 0.2%/10%. centa. Distributed in breast milk. Fetal
Vasocidin: prednisoLONE/sulfaceta- cleft palate often occurs with chronic,
mide: 0.25%/10%. first-trimester use. Breastfeeding not
recommended. Children: Prolonged
uCLASSIFICATION treatment or high dosages may decrease
PHARMACOTHERAPEUTIC: Adrenal short-term growth rate, cortisol secre-
corticosteroid. CLINICAL: Anti-in- tion. Elderly: May be more susceptible
flammatory, immunosuppressant. to developing hypertension or osteopo-
rosis.
USES INTERACTIONS
Systemic: Endocrine, rheumatic, hema- DRUG: CYP3A4 inducers (e.g., carBA-
tologic disorders; collagen, respiratory, Mazepine, phenytoin, rifAMPin) may
neoplastic, GI diseases; allergic states; decrease effects. Live virus vaccines
acute or chronic solid organ rejection. increase vaccine side effects, potentiate
Ophthalmic: Treatment of conjunctivi- virus replication, decrease pt’s antibody
tis, corneal injury (from chemical/ther- response to vaccine. May increase effect
mal burns, foreign body). of warfarin. May decrease therapeu-
tic effect of aldesleukin. May increase
PRECAUTIONS hyponatremic effect of desmopressin.
Contraindications: Hypersensitivity to HERBAL: Echinacea may decrease level/
prednisoLONE. Acute superficial herpes effects. FOOD: None known. LAB VAL-
simplex keratitis, systemic fungal infec- UES: May increase serum glucose, lipids,

Canadian trade name Non-Crushable Drug High Alert drug


964 prednisoLONE
sodium, uric acid. May decrease serum acne, mood swings, increased appetite,
calcium, WBC, hypothalamic pituitary ad- facial flushing, delayed wound healing,
renal (HPA) axis function, potassium. increased susceptibility to infection, di-
arrhea, constipation. Occasional: Head-
AVAILABILITY (Rx) ache, edema, change in skin color,
Solution, Ophthalmic: 1%. Solution, frequent urination. Rare: Tachycardia,
Oral: 15 mg/5 mL, 5 mg/5 mL, 10 mg/5 allergic reaction (rash, urticaria), psy-
mL, 20 mg/5 mL. Suspension, Ophthal- chological changes, hallucinations, de-
mic: 1%,  0.12%. Syrup: 15 mg/5 mL. pression. Ophthalmic: Stinging/burn-
Tablets: 5 mg. ing, posterior subcapsular cataracts.
Tablets, Orally Disintegrating: 10
mg, 15 mg, 30 mg. ADVERSE EFFECTS/TOXIC
REACTIONS
ADMINISTRATION/HANDLING Long-term therapy: Hypocalcemia, hy-
pokalemia, muscle wasting (esp. arms,
PO legs), osteoporosis, spontaneous frac-
• Give with food or fluids to decrease GI tures, amenorrhea, cataracts, glaucoma,
side effects. peptic ulcer, HF, immunosuppression.
Orally Disintegrating Tablets
Abrupt withdrawal following long-
• Do not break, crush, or divide tab- term therapy: Anorexia, nausea, fever,
lets. • Remove from blister just prior to headache, severe/sudden joint pain, re-
giving; place on tongue. • Pt may swal- bound inflammation, fatigue, weakness,
low whole or allow to dissolve in mouth lethargy, dizziness, orthostatic hypoten-
with/without water. sion. Sudden discontinuance may be fatal.

Ophthalmic NURSING CONSIDERATIONS


• For ophthalmic solution, shake well
P before using. • Instill drops into con- BASELINE ASSESSMENT
junctival sac, as prescribed. • Avoid Question medical history as listed in
touching applicator tip to conjunctiva Precautions. Obtain baselines for height,
to avoid contamination. weight, B/P, serum glucose, electrolytes.
Check results of initial tests (tuberculosis
INDICATIONS/ROUTES/DOSAGE [TB] skin test, X-rays, ECG).
Usual Dosage INTERVENTION/EVALUATION
PO: ADULTS, ELDERLY: 5–60 mg/day in
divided doses. CHILDREN: 0.1–2 mg/kg/ Monitor B/P, weight, serum electrolytes,
day in 3–4 divided doses. glucose, results of bone mineral density
test, height, weight in children. Be alert
Treatment of Conjunctivitis, Corneal Injury to infection (sore throat, fever, vague
Ophthalmic: ADULTS, ELDERLY, CHIL- symptoms); assess oral cavity daily for
DREN: 1–2 drops every hr during day signs of Candida infection. Monitor for
and q2h during night. After response, symptoms of adrenal insufficiency, im-
decrease dosage to 1 drop q4h, then 1 munosuppression.
drop 3–4 times/day. PATIENT/FAMILY TEACHING
Dosage in Renal/Hepatic Impairment • Report fever, sore throat, muscle aches,
No dose adjustment. sudden weight gain, swelling, loss of
appetite, fatigue. • Avoid alcohol, limit
SIDE EFFECTS caffeine. • Maintain fastidious oral hy-
Frequent: Insomnia, heartburn, nervous- giene. • Do not abruptly discontinue
ness, abdominal distention, diaphoresis, without physician’s approval. • Avoid

underlined – top prescribed drug


predniSONE 965
exposure to chickenpox, measles. at risk for hyperglycemia (e.g., diabetes,
• Long-term use may significantly in- recent surgery).
crease risk of serious infections.
ACTION
Inhibits accumulation of inflammatory
cells at inflammation sites, phagocyto-
predniSONE sis, lysosomal enzyme release/synthesis,
release of mediators of inflammation.
pred-ni-sone Therapeutic Effect: Prevents/sup-
(Apo-PredniSONE , PredniSONE presses cell-mediated immune reactions.
Intensol, Rayos, Winpred ) Decreases/prevents tissue response to
Do not confuse predniSONE inflammatory process.
with methylPREDNISolone, pra-
zosin, prednisoLONE, PriLOSEC, PHARMACOKINETICS
primidone, or promethazine. Well absorbed from GI tract. Protein
uCLASSIFICATION binding: 70%–90%. Widely distributed.
Metabolized in liver, converted to pred-
PHARMACOTHERAPEUTIC: Adrenal nisoLONE. Primarily excreted in urine.
corticosteroid. CLINICAL: Anti-in- Not removed by hemodialysis. Half-
flammatory, immunosuppressant. life: 2.5–3.5 hrs.

USES LIFESPAN CONSIDERATIONS


Substitution therapy in deficiency Pregnancy/Lactation: Crosses pla-
states: Acute or chronic adrenal insuf- centa. Distributed in breast milk. Fetal
ficiency, congenital adrenal hyperplasia, cleft palate often occurs with chronic,
adrenal insufficiency secondary to pitu- first trimester use. Breastfeeding not
itary insufficiency. Nonendocrine dis- recommended. Children: Prolonged P
orders: Arthritis, rheumatic carditis; al- treatment or high dosages may decrease
lergic, collagen, intestinal tract, multiple short-term growth rate, cortisol secre-
sclerosis exacerbations; liver, ocular, re- tion. Elderly: May be more susceptible
nal, skin diseases; bronchial asthma, ce- to developing hypertension or osteopo-
rebral edema, malignancies. OFF-LABEL: rosis.
Prevention of postherpetic neuralgia, re-
lief of acute pain in pts with herpes zoster, INTERACTIONS
autoimmune hepatitis. DRUG: CYP3A4 inducers (e.g., carBA-
Mazepine, phenytoin, rifAMPin) may
PRECAUTIONS decrease effects. Live virus vaccines
Contraindications: Hypersensitivity to may increase vaccine side effects, po-
predniSONE. Acute superficial herpes tentiate virus replication, decrease pt’s
simplex keratitis, systemic fungal infec- antibody response to vaccine. May in-
tions, varicella, administration of live or crease effect of warfarin. May decrease
attenuated virus vaccines. Cautions: Hy- therapeutic effect of aldesleukin. May
perthyroidism, cirrhosis, ocular herpes increase hyponatremic effect of des-
simplex, respiratory tuberculosis, un- mopressin. HERBAL: Echinacea may
treated systemic infections, renal/hepatic decrease therapeutic effect. FOOD: None
impairment, following acute MI, cata- known. LAB VALUES: May increase se-
racts, glaucoma, seizures, peptic ulcer rum glucose, lipids, sodium, uric acid.
disease, osteoporosis, myasthenia gra- May decrease serum calcium, potassium,
vis, hypertension, HF, ulcerative colitis, WBC, hypothalamic pituitary adrenal
thromboembolic disorders, elderly, pts (HPA) axis function.
Canadian trade name Non-Crushable Drug High Alert drug
966 pregabalin

AVAILABILITY (Rx) drawal following long-term therapy:


Solution, Oral: 1 mg/mL. Solution, Oral Anorexia, nausea, fever, headache, re-
Concentrate: (Prednisone Intensol): 5 bound inflammation, fatigue, weakness,
mg/mL. Tablets: 1 mg, 2.5 mg, 5 mg, 10 lethargy, dizziness, orthostatic hypoten-
mg, 20 mg, 50 mg. sion. Sudden discontinuance may be fatal.
Tablet, Delayed-Release: (Rayos): 1 NURSING CONSIDERATIONS
mg, 2 mg, 5 mg.
BASELINE ASSESSMENT
ADMINISTRATION/HANDLING Question medical history as listed in
PO Precautions. Obtain baselines for height,
• Give with food or fluids to decrease GI weight, B/P, serum glucose, electrolytes.
side effects. • Give single doses before Check results of initial tests (tuberculosis
9 AM, multiple doses at evenly spaced [TB] skin test, X-rays, ECG).
intervals. • Give delayed-release tablet
INTERVENTION/EVALUATION
whole; do not break, crush, dissolve, or
divide. Monitor B/P, serum electrolytes, glu-
cose, results of bone mineral density
INDICATIONS/ROUTES/DOSAGE test, height, weight in children. Be alert
Note: Dose dependent upon condition to infection (sore throat, fever, vague
treated, pt response rather than by rigid symptoms); assess oral cavity daily for
adherence to age, weight, or body surface signs of Candida infection. Monitor for
area. symptoms of adrenal insufficiency, im-
munosuppression.
Usual Dosage
PATIENT/FAMILY TEACHING
PO: ADULTS, ELDERLY: 10–60 mg/day in
divided doses. Range: 2.5–100 mg/day. • Report fever, sore throat, muscle aches,
CHILDREN: 0.05–2 mg/kg/day in 1–4 di- sudden weight gain, swelling, loss of ap-
P vided doses. petite, or fatigue. • Avoid alcohol, mini-
mize use of caffeine. • Report symptoms
Dosage in Renal/Hepatic Impairment of elevated blood sugar levels (blurred vi-
No dose adjustment. sion, headache, increased thirst, frequent
urination). • Maintain strict oral hy-
SIDE EFFECTS giene. • Do not abruptly discontinue
Frequent: Insomnia, heartburn, nervous- without physician’s approval. • Avoid
ness, abdominal distention, diaphoresis, exposure to chickenpox, mea-
acne, mood swings, increased appetite, sles. • Long-term use may significantly
facial flushing, delayed wound healing, increase risk of serious infections.
increased susceptibility to infection, di-
arrhea, constipation. Occasional: Head-
ache, edema, change in skin color,
frequent urination. Rare: Tachycardia, pregabalin
allergic reaction (rash, urticaria), psy-
chological changes, hallucinations, de- pre-gab-a-lin
pression. (Lyrica, Lyrica CR)
ADVERSE EFFECTS/TOXIC uCLASSIFICATION
REACTIONS PHARMACOTHERAPEUTIC: GABA
Long-term therapy: Muscle wasting analogue. CLINICAL: Anticon-
(esp. in arms, legs), osteoporosis, spon- vulsant, antineuralgic, analgesic
taneous fractures, amenorrhea, cataracts, (Schedule V).
glaucoma, peptic ulcer, HF. Abrupt with-
underlined – top prescribed drug
pregabalin 967

USES AVAILABILITY (Rx)


Lyrica: Adjunctive therapy in treatment 20 mg/mL.
Solution, Oral:
of partial-onset seizures. Management 25 mg, 50 mg,
Capsules: (Lyrica):
of neuropathic pain associated with dia- 75 mg, 100 mg, 150 mg, 200 mg, 225
betic peripheral neuropathy or spinal mg, 300 mg.
cord injury. Management of postherpetic Tablet, Extended-Release: (Lyrica
neuralgia. Management of fibromyalgia. CR): 82.5 mg, 165 mg, 330 mg.
Lyrica CR: Management of neuropathic
pain associated with diabetic peripheral ADMINISTRATION/HANDLING
neuropathy, postherpetic neuralgia. • Give without regard to food. • Ad-
PRECAUTIONS minister whole; do not break, crush, or
open capsule. • Lyrica CR: Give once
Contraindications: Hypersensitivity to daily in evening. • Discontinue pregab-
pregabalin. Cautions: HF, renal impair- alin gradually over at least 1 wk. • Ad-
ment, cardiovascular disease, diabetes, minister whole; do not break, cut, crush,
history of angioedema, pts at risk for or divide. Tablet cannot be chewed.
suicide. Concurrent use of thiazolidine
antidiabetics (e.g., Actos). INDICATIONS/ROUTES/DOSAGE
ACTION Partial-Onset Seizures
PO: ADULTS, ELDERLY: Initially, 75 mg twice
Binds to calcium channel sites in CNS tis-
sue, inhibiting excitatory neurotransmitter daily or 50 mg 3 times/day. May increase dose
release. Exerts antinociceptive, anticon- based on tolerability/effect. Maximum: 600
vulsant activity. Therapeutic Effect: De- mg/day. ADOLESCENTS, CHILDREN, INFANTS
WEIGHING 30 KG OR MORE: Initially, 2.5 mg/
creases symptoms of painful peripheral
neuropathy; decreases frequency of partial kg/day in 2 or 3 divided doses. May increase
seizures. wkly based on clinical response and tolerabil-
ity. Maximum: 10 mg/kg/day (not to exceed P
PHARMACOKINETICS 600 mg/day). LESS THAN 30 KG: Initially, 3.5
Well absorbed following PO administra- mg/kg/day in 2 or 3 divided doses. May in-
tion. Excreted in urine unchanged. Half- crease wkly based on clinical response and
life: 6 hrs. tolerability. Maximum: 14 mg/kg/day.
Neuropathic Pain (Diabetes-Associated)
LIFESPAN CONSIDERATIONS PO: ADULTS, ELDERLY: Initially, 25–75
Pregnancy/Lactation: Increased mg/day once daily or in 2–3 divided
risk of fetal skeletal abnormalities. Un- doses. May increase within 1 wk based
known if distributed in breast milk. Chil- on response and tolerability. Maximum:
dren: Safety and efficacy not established. 300–450 mg/day.
Elderly: Age-related renal impairment PO: (Lyrica CR): ADULTS, ELDERLY: Initially,
may require dosage adjustment. 165 mg once daily. May increase to 330 mg/
day within 1 wk. Maximum: 330 mg/day.
INTERACTIONS
DRUG: Alcohol, CNS depressants Postherpetic Neuralgia, Neuropathic Pain
(e.g., LORazepam, morphine, zol- Associated with Spinal Cord Injury
pidem) may increase sedative effect. PO: ADULTS, ELDERLY: Initially, 75 mg
HERBAL: Herbals with sedative prop- twice daily or 50 mg 3 times/day. May
erties (e.g., chamomile, kava kava, increase to 300 mg/day within 1 wk. May
valerian) may increase CNS depression. further increase to 600 mg/day after 2–4
FOOD: None known. LAB VALUES: May wks. Maximum: 600 mg/day.
increase CPK. May cause mild PR interval PO: (Lyrica CR): ADULTS, ELDERLY: Ini-
prolongation. May decrease platelet count. tially, 165 mg once daily. May increase
Canadian trade name Non-Crushable Drug High Alert drug
968 primidone
to 330 mg/day within 1 wk. May further NURSING CONSIDERATIONS
increase to 660 mg once daily after 2–4
wks. Maximum: 660 mg/day. BASELINE ASSESSMENT
Seizure: Review history of seizure dis-
Fibromyalgia order (type, onset, intensity, frequency,
PO: ADULTS, ELDERLY: Initially, 75 mg duration, LOC). Pain: Assess onset, type,
twice daily. May increase to 150 mg twice location, and duration of pain.
daily within 1 wk. Maximum: 225 mg
twice daily. INTERVENTION/EVALUATION
Provide safety measures as needed. Assess
Dosage in Renal Impairment for seizure activity. Assess for clinical im-
Creatinine provement; record onset of relief of pain.
Clearance Daily Dosage Assess for peripheral edema. Question for
30–60 mL/min 75–300 mg in 2–3 changes in visual acuity. Monitor weight.
divided doses
15–29 mL/min 25–150 mg in 1 or 2 PATIENT/FAMILY TEACHING
doses • Do not abruptly stop taking drug; sei-
Less than 15 mL/ 25–75 mg once
zure frequency may be increased. • Avoid
min daily
tasks that require alertness, motor skills
until response to drug is estab-
Dosage for Hemodialysis lished. • Avoid alcohol. • Carry identi-
b ALERT c Take supplemental dose im- fication card, bracelet to note seizure dis-
mediately following dialysis. order, anticonvulsant therapy.
Supplemental
Daily Dosage Dosage
25 mg Single dose of 25
mg or 50 mg primidone
P 25–50 mg Single dose of 50
mg or 75 mg prim-i-done
75 mg Single dose of 100 (Apo-Primidone , Mysoline)
mg or 150 mg Do not confuse primidone with
predniSONE or pyridoxine.
Dosage in Hepatic Impairment
No dose adjustment. uCLASSIFICATION
PHARMACOTHERAPEUTIC: Barbitu-
SIDE EFFECTS rate. CLINICAL: Anticonvulsant.
Frequent (32%–12%): Dizziness, drowsiness,
ataxia, peripheral edema. Occasional (12%–
5%): Weight gain, blurred vision, diplopia, USES
difficulty with concentration, attention, cog- Management of psychomotor, general-
nition; tremor, dry mouth, headache, consti- ized tonic-clonic (grand mal), and focal
pation, asthenia. Rare (4%–2%): Abnormal seizures. OFF-LABEL: Treatment of essen-
gait, confusion, incoordination, twitching, tial tremor (familial tremor).
flatulence, vomiting, edema, myopathy.
PRECAUTIONS
ADVERSE EFFECTS/TOXIC Contraindications: Hypersensitivity to
REACTIONS primidone, PHENobarbital; porphyria.
Abrupt withdrawal increases risk of Cautions: Renal/hepatic impairment,
seizure frequency in pts with seizure pulmonary insufficiency, elderly pts, de-
disorders; withdraw gradually over a bilitated pts, children, hypoadrenalism,
minimum of 1 wk. May increase risk of pts at risk for suicidal thoughts/behavior,
suicidal thoughts and behavior. depression, history of drug abuse.
underlined – top prescribed drug
primidone 969

ACTION 4–6: 100–125 mg twice daily. Days


Decreases neuron excitability. Raises 7–9: 100–125 mg 3 times/day. Usual
seizure threshold. Therapeutic Ef- dose: 750–1,500 mg/day in 3–4 di-
fect: Reduces seizure activity. vided doses. Maximum: 2 g/day. CHIL-
DREN YOUNGER THAN 8 YRS: Initially, 50
PHARMACOKINETICS mg/day at bedtime for days 1–3. Days
Rapidly, usually completely absorbed fol- 4–6: 50 mg twice daily. Days 7–9: 100
lowing PO administration. Protein binding: mg twice daily. Usual dose: 10–25 mg/
99%. Metabolized in liver to PHENobarbital. kg/day (375–750 mg) in 3–4 divided
Minimal excretion in urine. Half-life: 3–6 doses. NEONATES: 12–20 mg/kg/day in
hrs. (PHENobarbital: 2–5 days.) divided doses 2–4 times/day.

LIFESPAN CONSIDERATIONS Dosage in Renal Impairment


Creatine Clearance Interval
Pregnancy/Lactation: Crosses pla-
centa; distributed in breast milk. Chil- 50 mL/min or greater q12h
10–49 mL/min q12–24h
dren/Elderly: May produce paradoxi-
Less than 10 mL/min q24h
cal excitement, restlessness. Hemodialysis (HD) Administer dose
post-HD
INTERACTIONS
DRUG: Alcohol, other CNS depres- Dosage in Hepatic Impairment
sants (e.g., LORazepam, morphine, No dose adjustment.
zolpidem) may increase effects. Val-
proic acid increases concentration, risk SIDE EFFECTS
of toxicity. Strong CYP2C19 inducers Frequent: Ataxia, dizziness. Occasional:
(e.g., carBAMazepine, rifAMPin) may Anorexia, drowsiness, altered mental
decrease concentration/effect. Strong ­status, nausea, vomiting, paradoxical ex-
CYP2C19 inhibitors (e.g., FLUox- citement. Rare: Rash.
etine, fluvoxaMINE) may increase P
concentration/effect. May decrease effect ADVERSE EFFECTS/TOXIC
of dolutegravir, oral contraceptives, REACTIONS
tenofovir, voriconazole, warfarin. Abrupt withdrawal after prolonged ther-
HERBAL: Herbals with sedative prop- apy may produce effects ranging from
erties (e.g., chamomile, kava kava, markedly increased dreaming, night-
valerian) may increase CNS depression. mares, insomnia, tremor, diaphoresis,
FOOD: None known. LAB VALUES: May vomiting to hallucinations, delirium, sei-
decrease serum bilirubin. Therapeutic zures, status epilepticus. Skin eruptions
serum level: 4–12 mcg/mL; toxic se- may appear as hypersensitivity reaction.
rum level: greater than 12 mcg/mL. Blood dyscrasias, hepatic disease, hy-
pocalcemia occur rarely. Overdose pro-
AVAILABILITY (Rx) duces cold/clammy skin, hypothermia,
Tablets: 50 mg, 250 mg. severe CNS depression, followed by high
fever, coma. May increase risk of suicidal
ADMINISTRATION/HANDLING thoughts and behavior.
PO
• Give with food to minimize GI effects. NURSING CONSIDERATIONS
INDICATIONS/ROUTES/DOSAGE BASELINE ASSESSMENT
Seizure Control Review history of seizure disorder (inten-
PO: ADULTS, ELDERLY, CHILDREN 8 YRS sity, frequency, duration, LOC). Observe
AND OLDER: Initially, 100–125 mg/ frequently for recurrence of seizure activ-
day at bedtime for days 1–3. Days ity. Initiate seizure precautions.
Canadian trade name Non-Crushable Drug High Alert drug
970 prochlorperazine
INTERVENTION/EVALUATION 9 kg. Postoperative nausea/vomiting fol-
Monitor for changes in behavior, de- lowing pediatric surgery. Cautions: His-
pression, suicidal ideation. Monitor tory of seizures, Parkinson’s disease,
CBC, neurologic status (frequency, dura- elderly, pts at risk for pneumonia, severe
tion, severity of seizures). Monitor for renal/hepatic impairment, decreased GI
therapeutic serum level: 4–12 mcg/ motility, urinary retention, visual prob-
mL; toxic serum level: more than 12 lems, narrow-angle glaucoma, paralytic
mcg/mL. ileus, myasthenia gravis, cerebrovascu-
lar/cardiovascular disease.
PATIENT/FAMILY TEACHING
• Do not abruptly discontinue medica- ACTION
tion after long-term use (may precipitate Acts centrally to inhibit/block DOPamine
seizures). • Strict maintenance of drug receptors in brain, including the chemo-
therapy is essential for seizure con- receptor trigger zone. Therapeutic Ef-
trol. • Avoid tasks that require alertness, fect: Relieves nausea/vomiting.
motor skills until response to drug is es-
tablished; drowsiness usually disappears PHARMACOKINETICS
during continued therapy. • Slowly go Route Onset* Peak Duration
from lying to standing. • Avoid alco- PO 30–40 N/A 3–4 hrs
hol. • Report depression, thoughts of min
suicide, unusual changes in behavior. IM 10–20 N/A 4–6 hrs
min
Rectal 60 min N/A 12 hrs

prochlorperazine *As an antiemetic.

proe-klor-per-a-zeen Variably absorbed after PO administra-


(Compro) tion. Widely distributed. Metabolized in
P liver, GI mucosa. Primarily excreted in
j BLACK BOX ALERT jIncreased
risk for death in elderly with urine. Unknown if removed by hemodi-
dementia-related psychosis. alysis. Half-life: PO: 3–5 hrs, IV: 7 hrs.
Do not confuse prochlorpera-
zine with chlorproMAZINE. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Crosses pla-
uCLASSIFICATION centa. Distributed in breast milk. Chil-
PHARMACOTHERAPEUTIC: Pheno- dren: Safety and efficacy not established
thiazine. CLINICAL: Antiemetic, first- in pts weighing less than 9 kg or younger
generation (typical) antipsychotic. than 2 yrs. Elderly: More susceptible
to orthostatic hypotension, anticholiner-
gic effects (e.g., dry mouth), sedation,
USES extrapyramidal symptoms (EPS); lower
Management of severe nausea/vomiting. dosage recommended.
OFF-LABEL: Behavioral syndromes in
INTERACTIONS
dementia, psychosis/agitation related to
Alzheimer’s dementia. DRUG: Alcohol, other CNS depres-
sants (e.g., LORazepam, morphine,
PRECAUTIONS zolpidem) may increase CNS, respira-
Contraindications: Hypersensitivity to tory depression, hypotensive effects.
prochlorperazine. Coma or presence Lithium may decrease absorption, pro-
of large amounts of CNS depressants duce adverse neurologic effects. May
(e.g., alcohol, opioids). Use in children increase concentration/effect of dofeti-
younger than 2 yrs or weighing less than lide. May increase arrhythmogenic
underlined – top prescribed drug
prochlorperazine 971
­effect of dronedarone. Aclidinium, DREN WEIGHING MORE THAN 39 KG: 5–10
ipratropium, tiotropium, umecli- mg q6–8h. Maximum: 40 mg/day. 19–
dinium may increase anticholinergic ef- 39 KG: 2.5 mg q8h or 5 mg q12h. Maxi-
fect. HERBAL: Kava kava may increase mum: 15 mg/day. 14–18 KG: 2.5 mg
adverse effects. FOOD: None known. LAB q8–12h. Maximum: 10 mg/day. 9–13
VALUES: None significant. KG: 2.5 mg q12–24h. Maximum: 7.5
mg/day.
AVAILABILITY (Rx) IV: ADULTS, ELDERLY: 2.5–10 mg. May
Injection Solution: 5 mg/mL. Supposi- repeat q3–4h. Maximum: 10 mg/dose
tories: (Compro): 25 mg. Tablets: 5 mg, or 40 mg/day.
10 mg. IM: ADULTS, ELDERLY: 5–10 mg q3–4h.
CHILDREN: 0.1–0.15 mg/kg/dose q8–
ADMINISTRATION/HANDLING 12h. Maximum single dose: 10 mg.
IV Rectal: ADULTS, ELDERLY: 25 mg twice
daily.
Rate of administration • May give by
IV push slowly. Maximum rate: 5 mg/min. Dosage in Renal/Hepatic Impairment
Storage • Store at room tempera- No dose adjustment.
ture. • Protect from light. • Clear or SIDE EFFECTS
slightly yellow solutions may be used.
Frequent: Drowsiness, hypotension, diz-
IM ziness, fainting (commonly occurring
• Inject deep IM into outer quadrant of after first dose, occasionally after sub-
buttocks. sequent doses, rarely with oral form).
Occasional: Dry mouth, blurred vision,
PO lethargy, constipation, diarrhea, myalgia,
• Should be administered with food or nasal congestion, peripheral edema, uri-
water. nary retention. P
Rectal ADVERSE EFFECTS/TOXIC
• Moisten suppository with cold water REACTIONS
before inserting well into rectum. Extrapyramidal symptoms (EPS) appear
dose related and are divided into three
IV INCOMPATIBILITIES categories: akathisia (e.g., inability to sit
Furosemide (Lasix), hydrocortisone, HY- still, tapping of feet), parkinsonian symp-
DROmorphone (Dilaudid), midazolam toms (mask-like face, tremors, shuffling
(Versed). gait, hypersalivation), acute dystonias
(torticollis [neck muscle spasm], opis-
IV COMPATIBILITIES thotonos [rigidity of back muscles],
Calcium gluconate, dexmedetomidine oculogyric crisis [rolling back of eyes]).
(Precedex), diphenhydrAMINE (Bena­ Dystonic reaction may produce diapho-
dryl), fentaNYL, heparin, metoclo- resis, pallor. Tardive dyskinesia (tongue
pramide (Reglan), morphine, potassium protrusion, puffing of cheeks, puckering
chloride, promethazine (Phenergan), of mouth) occurs rarely and may be ir-
propofol (Diprivan). reversible. Abrupt withdrawal after long-
term therapy may precipitate nausea,
INDICATIONS/ROUTES/DOSAGE vomiting, gastritis, dizziness, tremors.
Nausea/Vomiting Blood dyscrasias, particularly agranulo-
PO: ADULTS, ELDERLY:5–10 mg 3–4 cytosis, mild leukopenia, may occur. May
times/day. Maximum: 40 mg/day. CHIL- lower seizure threshold.

Canadian trade name Non-Crushable Drug High Alert drug


972 propafenone

NURSING CONSIDERATIONS USES


Immediate-Release: Treatment of life-
BASELINE ASSESSMENT threatening ventricular arrhythmias (e.g.,
Avoid skin contact with solution (con- sustained ventricular tachycardias). To
tact dermatitis). Antiemetic: Assess prolong time to recurrence of parox-
for dehydration (poor skin turgor, dry ysmal atrial fibrillation/flutter (PAF) or
mucous membranes, longitudinal fur- paroxysmal supraventricular tachycardia
rows in tongue). Antipsychotic: Assess (PSVT) in pts with disabling symptoms
behavior, appearance, emotional status, and without structural heart disease.
response to environment, speech pattern, Extended-Release: Prolong the time to
thought content. recurrence of atrial fibrillation/flutter or
INTERVENTION/EVALUATION
paroxysmal supraventricular tachycardia
in pts with disabling symptoms without
Monitor B/P for hypotension. Assess for structural heart disease. OFF-LABEL:
EPS. Monitor CBC for blood dyscrasias. Treatment following cardioversion of
Monitor for fine tongue movement (may recent-onset atrial fibrillation; supra-
be early sign of tardive dyskinesia). Su- ventricular tachycardia in pts with Wolff-
pervise suicidal-risk pt closely during Parkinson-White syndrome.
early therapy (as depression lessens,
energy level improves, increasing sui- PRECAUTIONS
cide potential). Assess for therapeutic Contraindications: Hypersensitivity to
response (interest in surroundings, im- propafenone. Sinus bradycardia, bron-
provement in self-care, increased ability chospastic disorders or severe obstructive
to concentrate, relaxed facial expression pulmonary disease, cardiogenic shock,
or relief of nausea, vomiting). uncorrected electrolyte imbalance, sino-
PATIENT/FAMILY TEACHING atrial, AV, intraventricular impulse gen-
• Limit caffeine. • Avoid alco- eration or conduction disorders (e.g.,
P sick sinus syndrome, AV block) without
hol. • Avoid tasks requiring alertness,
motor skills until response to drug is es- pacemaker, uncompensated HF, marked
tablished (may cause drowsiness, im- hypotension. Cautions: Renal/hepatic im-
pairment). pairment, myasthenia gravis, concurrent
use of other medications that prolong QT
interval, hypokalemia, hypomagnesemia.
ACTION
propafenone Blocks fast inward sodium current.
proe-paf-e-nown Slows the rate of increase of the action
(Apo-Propafenone , Rythmol SR) potential (prolongs conduction veloc-
ity, refractory period). Therapeutic
j BLACK BOX ALERT j Mortality Effect: Suppresses arrhythmias.
or nonfatal cardiac arrest rate
(7.7% of pts) in asymptomatic
non–life-threatening ventricular ar- PHARMACOKINETICS
rhythmia pts with recent MI (more Nearly completely absorbed following PO
than 6 days but less than 2 yrs prior) administration. Protein binding: 85%–
reported.
97%. Metabolized in liver. Primarily ex-
uCLASSIFICATION creted in feces. Half-life: 2–10 hrs.
PHARMACOTHERAPEUTIC: Class 1c LIFESPAN CONSIDERATIONS
antiarrhythmic. CLINICAL: Antiar-
Pregnancy/Lactation: Crosses pla-
rhythmic.
centa, distributed in breast milk.

underlined – top prescribed drug


propafenone 973
Children: Safety and efficacy not es- Dosage in Renal Impairment
tablished. Elderly: No age-related pre- No dose adjustment.
cautions noted.
Dosage in Hepatic Impairment
INTERACTIONS Use caution.
DRUG: Amiodarone may affect cardiac SIDE EFFECTS
conduction, repolarization. May increase
effects of warfarin. CYP3A4 inhibitors Frequent (13%–7%): Dizziness, nausea,
(e.g., ketoconazole, erythromycin) vomiting, altered taste, constipation. Oc-
may increase concentration/toxicity. casional (6%–3%): Headache, dyspnea,
Strong CYP2D6 inhibitors (e.g., bu- blurred vision, dyspepsia. Rare (less than
PROPion, FLUoxetine) may increase 2%): Rash, weakness, dry mouth, diar-
concentration/effect. HERBAL: St. John’s rhea, edema, hot flashes.
wort may decrease concentration/effect.
FOOD: Grapefruit products may in- ADVERSE EFFECTS/TOXIC
crease concentration. LAB VALUES: May REACTIONS
cause ECG changes (e.g., QRS widening, May produce, worsen arrhythmias, HF.
PR interval prolongation), positive ANA Overdose may produce hypotension,
titer. drowsiness, bradycardia, atrioventricular
conduction disturbances.
AVAILABILITY (Rx)
Tablets: 150 mg, 225 mg, 300 mg. NURSING CONSIDERATIONS
Capsules, Extended-Release: 225 BASELINE ASSESSMENT
mg, 325 mg, 425 mg.
Correct electrolyte imbalance before ad-
ADMINISTRATION/HANDLING ministering medication. Obtain baseline
ECG. Screen for cardiac contraindica-
PO tions. P
• May take without regard to
food. • Give whole; do not break, INTERVENTION/EVALUATION
crush, divide, or open capsules. Assess pulse for quality, rhythm, rate.
Monitor ECG for cardiac performance
INDICATIONS/ROUTES/DOSAGE or changes, particularly widening of
Ventricular Arrhythmias, PAT, PSVT QRS, prolongation of PR interval. Ques-
PO: (Immediate-Release): ADULTS, tion for visual disturbances, headache,
ELDERLY: Initially, 150 mg q8h. May GI upset. Monitor fluid, serum elec-
increase at 3- to 4-day intervals to 225 trolyte levels. Monitor daily pattern of
mg q8h, then to 300 mg q8h. Maxi- bowel activity, stool consistency. Assess
mum: 900 mg/day. for dizziness, unsteadiness. Monitor
LFT. Monitor for therapeutic serum level
Atrial Fibrillation (Prevention of (0.06–1 mcg/mL).
Recurrence)
PO: (Immediate-Release): ADULTS, PATIENT/FAMILY TEACHING
ELDERLY: Initially, 150 mg q8h. May • Compliance with therapy regimen is
increase at 3- to 4-day intervals to essential to control arrhythmias. • Al-
225 mg q8h, then to 300 mg q8h. tered taste sensation may occur. • Re-
Maximum: 900 mg/day. (Extended-­ port headache, blurred vision. • Avoid
Release): ADULTS, ELDERLY: Initially, 225 tasks that require alertness, motor skills
mg q12h. May increase at 5-day intervals until response to drug is estab-
to 325 mg q12h. Maximum: 425 mg lished. • Report chest pain, difficulty
q12h. breathing, palpitations.

Canadian trade name Non-Crushable Drug High Alert drug


974 propofol

LIFESPAN CONSIDERATIONS
propofol Pregnancy/Lactation: Unknown if
proe-poe-fol drug crosses placenta. Distributed in
(Diprivan, Fresenius Propoven) breast milk. Not recommended for ob-
Do not confuse Diprivan with stetrics, breastfeeding mothers. Chil-
Diflucan or Ditropan, or propo- dren: Safety and efficacy not established.
fol with fospropofol. FDA-approved for use in pts 2 mos and
older. Elderly: No age-related precau-
uCLASSIFICATION tions noted; lower dosages recommended.
PHARMACOTHERAPEUTIC: Rapid- INTERACTIONS
acting general anesthetic. CLINI-
CAL: Sedative-hypnotic. DRUG: Alcohol, CNS depressants (e.g.,
LORazepam, morphine, zolpidem)
may increase CNS, respiratory depres-
USES sion, hypotensive effects. Antihyperten-
Induction/maintenance of anesthesia. sive medications (e.g., amLODIPine,
Continuous sedation in intubated and lisinopril, valsartan) may increase hy-
respiratory controlled adult pts in ICU. potensive effects. HERBAL: Herbals with
OFF-LABEL: Postop antiemetic, refractory sedative properties (e.g., chamomile,
status epilepticus. kava kava, valerian) may increase CNS
depression. Herbals with hypoten-
PRECAUTIONS sive properties (e.g., garlic, ginger,
gingko biloba) may increase effect.
Contraindications: Hypersensitivity to FOOD: None known. LAB VALUES: May
propofol, eggs, egg products, soybean increase serum triglycerides.
or soy products. Cautions: Hemody-
namically unstable pts, hypovolemia, AVAILABILITY (Rx)
P severe cardiac/respiratory disease, Injection Emulsion: 10 mg/mL.
elevated ICP, impaired cerebral circu-
lation, preexisting pancreatitis, hyper- ADMINISTRATION/HANDLING
lipidemia, history of epilepsy, seizure IV
disorder, elderly pts, debilitated pts, pts
allergic to peanuts. b ALERT c Do not give through same IV
line with blood or plasma.
ACTION Reconstitution • May give undiluted,
Causes CNS depression through agonist or dilute only with D5W. • Do not dilute
action of GABA receptors. Therapeutic to concentration less than 2 mg/mL (4 mL
Effect: Produces hypnosis rapidly. D5W to 1 mL propofol yields 2 mg/mL).
Rate of administration • Too-rapid
PHARMACOKINETICS IV administration may produce marked
Route Onset Peak Duration severe hypotension, respiratory depres-
sion, irregular muscular move-
IV 40 sec N/A 3–10 min
ments. • Observe for signs of extrava-
Rapidly, extensively distributed. Pro- sation (pain, discolored skin patches,
tein binding: 97%–99%. Metabolized white or blue color to peripheral IV site
in liver. Primarily excreted in urine. area, delayed onset of drug action).
Unknown if removed by hemodialysis. Storage • Store at room tempera-
Rapid awakening can occur 10–15 ture. • Discard unused portions. • Do
min after discontinuation. Half-life: not use if emulsion separates. • Shake
3–12 hrs. well before using.

underlined – top prescribed drug


propofol 975

IV INCOMPATIBILITIES Dosage in Renal/Hepatic Impairment


Amikacin (Amikin), amphotericin B com- No dose adjustment.
plex (Abelcet, AmBisome, Amphotec), SIDE EFFECTS
bretylium (Bretylol), calcium chloride,
ciprofloxacin (Cipro), diazePAM (Va- Frequent: Involuntary muscle movements,
lium), digoxin (Lanoxin), DOXOrubicin apnea (common during induction; often
(Adriamycin), gentamicin (Garamycin), lasts longer than 60 sec), hypotension, nau-
methylPREDNISolone (SOLU-Medrol), sea, vomiting, IV site burning/stinging. Oc-
casional: Twitching, thrashing, headache,
minocycline (Minocin), phenytoin (Dilan-
tin), tobramycin (Nebcin), verapamil dizziness, bradycardia, hypertension, fever,
(Isoptin). abdominal cramps, paresthesia, coldness,
cough, hiccups, facial flushing, green-tinted
urine. Rare: Rash, dry mouth, agitation,
IV COMPATIBILITIES confusion, myalgia, thrombophlebitis.
Acyclovir (Zovirax), bumetanide (Bu-
mex), calcium gluconate, cefTAZidime ADVERSE EFFECTS/TOXIC
(Fortaz), dexmedetomidine (Prece- REACTIONS
dex), DOBUTamine (Dobutrex), DOPa- Continuous infusion or repeated intermit-
mine (Intropin), enalapril (Vasotec), tent infusions of propofol may result in
fentaNYL, heparin, insulin, labetalol extreme drowsiness, respiratory depres-
(Normodyne, Trandate), lidocaine, sion, circulatory depression, delirium.
LORazepam (Ativan), magnesium, mil- Too-rapid IV administration may produce
rinone (Primacor), nitroglycerin, nor- severe hypotension, respiratory depres-
epinephrine (Levophed), potassium sion, involuntary muscle movements. Pt
chloride, vancomycin (Vancocin). may experience acute allergic reaction,
characterized by abdominal pain, anxiety,
INDICATIONS/ROUTES/DOSAGE restlessness, dyspnea, erythema, hypo-
Anesthesia
tension, pruritus, rhinitis, urticaria. May P
IV infusion: ADULTS, ELDERLY: Induc- cause propofol infusion syndrome, a col-
tion, 2–2.5 mg/kg (approximately 40 mg lection of metabolic disorders and organ
q10sec until onset of anesthesia). Main- system failures including metabolic acido-
tenance: Initially, 100–200 mcg/kg/ sis, hyperkalemia, rhabdomyolysis, hepa-
min or 6–12 mg/kg/hr for 10–15 min. tomegaly; cardiac, renal failure.
Usual maintenance infusion: 50–100 NURSING CONSIDERATIONS
mcg/kg/min or 3–6 mg/kg/hr. CHILDREN
3–16 YRS: Induction, 2.5–3.5 mg/kg over BASELINE ASSESSMENT
20–30 sec, then infusion of 125–300 Resuscitative equipment, suction, O2
mcg/kg/min or 7.5–18 mg/kg/hr. must be available. Obtain vital signs be-
Sedation in ICU fore administration.
IV infusion: ADULTS, ELDERLY: Initially, 5
INTERVENTION/EVALUATION
mcg/kg/min (0.3 mg/kg/hr); increase by
increments of 5–10 mcg/kg/min (0.3– Observe pt for signs of wakefulness, agita-
0.6 mg/kg/hr) q5–10 min until desired tion. Monitor respiratory rate, B/P, heart
sedation level achieved. Usual mainte- rate, O2 saturation, ABGs, depth of seda-
nance: 5–50 mcg/kg/min (0.3–3 mg/ tion, serum lipid, triglycerides (if used
kg/hr). Reduce dose after adequate seda- longer than 24 hrs). May change urine
tion established, and adjust to response. color to green. If continuous high-dose
Daily interruption with retitration (seda- infusions do not properly induce seda-
tion vacation) recommended to minimize tion, consider additional sedatives (e.g.,
­prolonged sedative effects. opioids, hypnotics, benzodiazepines) to
achieve desired response.
Canadian trade name Non-Crushable Drug High Alert drug
976 propranolol

PRECAUTIONS
propranolol Contraindications: Hypersensitivity to
propranolol. Bronchial asthma, severe si-
proe-pran-oh-lol
nus bradycardia, cardiogenic shock, sick
(Hemangeol, Inderal LA, Inderal XL,
sinus syndrome, heart block greater than
InnoPran XL)
first-degree (unless pt has functional pace-
j BLACK BOX ALERT j Severe maker), uncompensated HF. Hemangeol
angina exacerbation, MI, ventricu-
lar arrhythmias may occur in angina (Additional): Premature infants with
pts after abrupt discontinuation; corrected age younger than 5 wks, in-
must taper gradually over 1–2 wks. fants weighing less than 2.5 kg; history of
Do not confuse Inderal LA with bronchospasm, bradycardia (less than 80
Adderall, Imdur, Isordil, or beats/min), B/P less than 50/30 mm Hg,
Toradol, or propranolol with pheochromocytoma. Cautions: Diabetes,
Pravachol. renal/hepatic impairment, Raynaud’s dis-
ease, hyperthyroidism, myasthenia gravis,
FIXED-COMBINATION(S) psychiatric disease, bronchospastic dis-
Inderide: propranolol/hydroCHLO- ease, elderly pts, history of severe anaphy-
ROthiazide (a diuretic): 40 mg/25 laxis to allergens.
mg, 80 mg/25 mg. Inderide LA:
propranolol/hydroCHLOROthiazide (a ACTION
diuretic): 80 mg/50 mg, 120 mg/50 Blocks beta1-, beta2-adrenergic recep-
mg, 160 mg/50 mg. tors. Therapeutic Effect: Slows heart
rate; decreases B/P, myocardial contrac-
uCLASSIFICATION tility, myocardial oxygen demand.
PHARMACOTHERAPEUTIC: Non-
selective beta-adrenergic blocker. PHARMACOKINETICS
CLINICAL: Antihypertensive, an- Route Onset Peak Duration
P
tianginal, antiarrhythmic, antimi- PO 1–2 hrs N/A 6 hrs
graine.
Well absorbed from GI tract. Protein
binding: 93%. Widely distributed. Me-
USES tabolized in liver. Primarily excreted in
Treatment of angina pectoris, supra- urine. Not removed by hemodialysis.
ventricular arrhythmias, essential Half-life: 4–6 hrs.
tremors, hypertension, ventricular
LIFESPAN CONSIDERATIONS
tachycardia, symptomatic treatment
of obstructive hypertrophic cardio- Pregnancy/Lactation: Crosses pla-
myopathy, treatment of proliferating centa. Distributed in breast milk. Avoid
infantile hemangioma requiring sys- use during first trimester. May produce
temic therapy, migraine headache low-birth-weight infants, bradycardia,
prophylaxis, pheochromocytoma, pre- apnea, hypoglycemia, hypothermia dur-
vention of MI. Hemangeol: Treatment ing delivery. Children: No age-related
of proliferating infantile hemangioma precautions noted. Elderly: Age-related
needing systemic therapy. OFF-LABEL: peripheral vascular disease may increase
Treatment adjunct for anxiety, tremor susceptibility to decreased peripheral
due to Parkinson’s disease, alco- circulation.
hol withdrawal, aggressive behavior,
INTERACTIONS
schizophrenia, antipsychotic-induced
akathisia, variceal hemorrhage, acute DRUG: Alpha2 agonists (e.g., cloNI-
panic. Dine) may increase AV-blocking effect.

underlined – top prescribed drug


propranolol 977
Strong CYP3A4 inducers (e.g., car- IV INCOMPATIBILITIES
BAMazepine, phenytoin, rifAMPin) Amphotericin B complex (Abelcet, AmBi-
may decrease concentration/effect. some, Amphotec).
Dronedarone, fingolimod, rivastig-
mine may increase bradycardic effect. IV COMPATIBILITIES
May increase vasoconstriction of er- Alteplase (Activase), heparin, milrinone
got derivatives (e.g., ergotamine). (Primacor), potassium chloride, propo-
HERBAL: Herbals with hypertensive fol (Diprivan).
properties (e.g., licorice, yohimbe)
or hypotensive properties (e.g., INDICATIONS/ROUTES/DOSAGE
garlic, ginger, ginkgo biloba) may Hypertension
alter effects. FOOD: None known. LAB PO: ADULTS, ELDERLY: (Immediate-Re-
VALUES: May increase serum antinu-
lease or Extended-Release): Initially,
clear antibody (ANA) titer, serum BUN, 80 mg/day. May increase at greater than
LDH, lipoprotein, alkaline phosphatase, or equal to 1-wk intervals prn based on
potassium, uric acid, ALT, AST, triglyc- patient response. Usual dosage range:
erides. 80–160 mg/day.
AVAILABILITY (Rx) Angina
Injection Solution: 1 mg/mL. Oral Solu- PO: ADULTS, ELDERLY: (Immediate-
tion: 20 mg/5 mL, 40 mg/5 mL. Oral Release): Initially, 80 mg/day. Increase
Solution: (Hemangeol): 4.28 mg/mL. dose as tolerated to desired effect. Range:
Tablets: 10 mg, 20 mg, 40 mg, 60 mg, 80–320 mg/day in 2–4 divided doses.
80 mg. PO: (Extended-Release [Inderal LA]):
Capsules, Sustained-Release: 60 mg, Initially, 80 mg/day. Increase dose as tol-
80 mg, 120 mg, 160 mg. erated to desired effect. Range: 80–320
mg/day.
P
ADMINISTRATION/HANDLING Arrhythmia
IV IV: ADULTS, ELDERLY: 1–3 mg. Repeat
q2–5min up to total of 5 mg. CHIL-
Reconstitution • Give undiluted for DREN: 0.01–0.15 mg/kg. May repeat
IV push. • For IV infusion, may dilute q6–8h. Maximum: Infants, 1 mg/
each 1 mg in 10 mL D5W. dose; children, 3 mg/dose.
Rate of administration • Do not ex- PO: ADULTS, ELDERLY: (Immediate-
ceed 1 mg/min injection rate. • For IV Release): 10–40 mg 3–4 times/day.
infusion, give over 30 min. CHILDREN: Initially, 0.5–1 mg/kg/day
Storage • Store at room tempera- in divided doses q6–8h. May increase
ture. • Once diluted, stable for 24 hrs q3days. Usual dosage: 2–4 mg/kg/day.
at room temperature. Maximum: 16 mg/kg/day or 60 mg/day.
PO Adjunct to Alpha-Blocking Agents to Treat
• May crush scored tablets. • Do not Pheochromocytoma
break, crush, or open extended- or sus- PO: ADULTS, ELDERLY: Initially, 10 mg
tained-release capsules. • Give immediate- q6h or 20 mg 3 times daily. Begin 3–4
release tablets on empty stomach. • Give days after initiation of an alpha-1 blocker
extended-release, sustained-­release without and adjust to goal heart rate up to 120
regard to food. mg/day in divided doses.

Canadian trade name Non-Crushable Drug High Alert drug


978 propranolol
Migraine Headache ADVERSE EFFECTS/TOXIC
PO: ADULTS, ELDERLY: (Immediate- REACTIONS
Release or Extended-Release): Ini­
Overdose may produce profound brady-
tially, 40–80 mg/day. May increase cardia, hypotension. Abrupt withdrawal
gradually based on response and tol- may result in diaphoresis, palpitations,
erability. Usual effective range: 40–160 headache, tremulousness. May precipi-
mg/day. CHILDREN 7 YRS AND OLDER: tate HF, MI in pts with cardiac disease,
(Immediate-Release): Initially, 10 mg
thyroid storm in pts with thyrotoxicosis,
daily. May increase at wkly intervals in peripheral ischemia in pts with existing
10 mg increments. Usual dose range: peripheral vascular disease. Hypogly-
10–20 mg 3 times/day. cemia may occur in pts with previously
controlled diabetes. Antidote: Glucagon
Reduction of Cardiovascular Mortality,
(see Appendix J for dosage).
Reinfarction in Pts with Previous MI
PO: ADULTS, ELDERLY: (Immediate-Re- NURSING CONSIDERATIONS
lease): Initially, 60–120 mg/day in 2–3
divided doses. May increase dose based BASELINE ASSESSMENT
on heart rate and BP up to 240 mg/day. Assess baseline renal function, LFT. Assess
B/P, apical pulse immediately before admin-
Essential Tremor istering drug (if pulse is 60/min or less or
PO: ADULTS, ELDERLY: (Immediate- systolic B/P is less than 90 mm Hg, withhold
Release or Extended-Release): Ini- medication, contact physician). Angina:
tially, 60–80 mg/day. May increase based Record onset, quality, radiation, location,
on response and tolerability. Usual dos- intensity, duration of anginal pain, precipi-
age range: 60–320 mg/day. tating factors (exertion, emotional stress).
Infantile Hemangioma INTERVENTION/EVALUATION
Note: Separate doses by at least 9 hrs Assess pulse for quality, regularity, bradycar-
P
during or after feeding. dia. Monitor ECG for cardiac arrhythmias.
PO: INFANTS 5 WKS TO 5 MOS: Initially, Assess fingers for color, numbness (Rayn-
0.15 mL/kg (0.6 mg/kg) twice daily. aud’s). Assess for evidence of HF (dyspnea
After 1 wk, increase to 0.3 mL/kg (1.1 [particularly on exertion or lying down],
mg/kg) twice daily. After 2 wks, increase night cough, peripheral edema, distended
to maintenance dose of 0.4 mL/kg (1.7 neck veins). Monitor I&O (increase in
mg/kg) twice daily. Maintain dose for weight, decrease in urinary output may indi-
6 months. Readjust dose as weight in- cate HF). Assess for rash, fatigue, behavioral
creases. changes. Therapeutic response time ranges
from a few days to several wks. Measure B/P
Dosage in Renal/Hepatic Impairment near end of dosing interval (determines if
Use caution. B/P is controlled throughout day).
SIDE EFFECTS PATIENT/FAMILY TEACHING
Frequent: Diminished sexual function, • Do not abruptly discontinue medica-
drowsiness, difficulty sleeping, unusual tion. • Compliance with therapy regi-
fatigue/weakness. Occasional: Bradycar- men is essential to control hypertension,
dia, depression, sensation of coldness in arrhythmia, anginal pain. • To avoid hy-
extremities, diarrhea, constipation, anxi- potensive effect, slowly go from lying to
ety, nasal congestion, nausea, vomiting. standing. • Avoid tasks that require
Rare: Altered taste, dry eyes, pruritus, par- alertness, motor skills until response to
esthesia. drug is established. • Report excessively

underlined – top prescribed drug


propylthiouracil 979
slow pulse rate (less than 50 beats/min), INTERACTIONS
peripheral numbness, dizziness. • Do DRUG: May increase concentration of
not use nasal decongestants, OTC cold digoxin. May decrease effect of oral
preparations (stimulants) without physi- anticoagulants (e.g., warfarin).
cian approval. • Restrict salt, alcohol HERBAL: None significant. FOOD: None
intake. known. LAB VALUES: May increase LDH,
serum alkaline phosphatase, bilirubin,
ALT, AST, prothrombin time.
propylthiouracil AVAILABILITY (Rx)
Tablets: 50 mg.
proe-pil-thye-oh-ure-a-sil
(Propyl-Thyracil ) ADMINISTRATION/HANDLING
j BLACK BOX ALERT jMay PO
cause severe hepatic injury, acute • Give with food.
hepatic failure, death.
Do not confuse propylthiouracil INDICATIONS/ROUTES/DOSAGE
with Purinethol.
Hyperthyroidism
uCLASSIFICATION PO: ADULTS, ELDERLY: Initially, 300–
400 mg/day (ELDERLY: 150–300 mg/
PHARMACOTHERAPEUTIC: Thiourea
day) in divided doses q8h. Mainte-
derivative. CLINICAL: Antithyroid
nance: 100–150 mg/day in divided
agent.
doses q8–12h.
Dosage in Renal/Hepatic Impairment
USES No dose adjustment.
Palliative treatment of hyperthyroidism in
pts with Graves’ disease or toxic multi- SIDE EFFECTS P
nodular goiter or intolerant of methima- Frequent: Urticaria, rash, pruritus, nau-
zole. Amelioration of hyperthyroid symp- sea, skin pigmentation, hair loss, head-
toms in preparation for thyroidectomy or ache, paresthesia. Occasional: Drowsi-
radioactive iodine therapy. OFF-LABEL: ness, lymphadenopathy, vertigo. Rare:
Management of thyrotoxic crises, Graves’ Drug fever, lupus-like syndrome.
disease, thyroid storm.
ADVERSE EFFECTS/TOXIC
PRECAUTIONS REACTIONS
Contraindications: Hypersensitivity to Agranulocytosis (may occur as long as 4
propylthiouracil. Cautions: In combina- mos after therapy), pancytopenia, fatal
tion with other agranulocytosis-inducing hepatitis have occurred.
drugs.
ACTION NURSING CONSIDERATIONS
Blocks conversion of thyroxine to tri- BASELINE ASSESSMENT
iodothyronine in peripheral tissues. Obtain baseline weight, pulse. Obtain
Therapeutic Effect: Inhibits synthesis baseline T3, T4, TSH level, LFT.
of thyroid hormone.
INTERVENTION/EVALUATION
PHARMACOKINETICS Monitor pulse, weight daily. Check for
Readily absorbed from GI tract. Protein skin eruptions, pruritus, swollen lymph
binding: 80%. Metabolized in liver. Ex- glands. Be alert for signs, symptoms of
creted in urine. Half-life: 1.5–5 hrs. hepatic injury, hepatitis (nausea, vom-
Canadian trade name Non-Crushable Drug High Alert drug
980 pyrazinamide
iting, drowsiness, jaundice). Monitor drug concentration at infection site, sus-
hematology results for bone marrow sup- ceptibility of infecting bacteria.
pression; observe for signs of infection,
bleeding. PHARMACOKINETICS
Well absorbed from GI tract. Protein
PATIENT/FAMILY TEACHING
binding: 5%–10%. Widely distributed.
• Space doses evenly around the Metabolized in liver. Excreted in urine.
clock. • Take resting pulse daily. Half-life: 9–10 hrs.
• Report pulse rate less than 60 beats/
min. • Seafood, iodine products may LIFESPAN CONSIDERATIONS
be restricted. • Report fever, sore Pregnancy/Lactation: Unknown if
throat, yellowing of skin/eyes, unusual drug crosses placenta or is distributed
bleeding/bruising immediately. • Re- in breast milk. Children: Safety and ef-
port sudden or continuous weight gain, ficacy not established. Elderly: No age-
cold intolerance, depression. related precautions noted.
INTERACTIONS
DRUG: May diminish effect of BCG (intra-
pyrazinamide vesical). RifAMPin may increase risk of
hepatoxicity. HERBAL: None significant.
peer-a-zin-a-mide FOOD: None known. LAB VALUES: May
(Tebrazid ) increase serum ALT, AST, uric acid.
FIXED-COMBINATION(S) AVAILABILITY (Rx)
Rifater: pyrazinamide/isoniazid/ Tablets: 500 mg.
rifAMPin (an antitubercular): 300
mg/50 mg/120 mg. INDICATIONS/ROUTES/DOSAGE
P
uCLASSIFICATION Tuberculosis (in Combination With Other
PHARMACOTHERAPEUTIC: Synthetic Antituberculars)
pyrazine analogue. CLINICAL: An- PO: ADULTS: Based on lean body
titubercular. weight. 40–55 KG: 1,000 mg once daily or
1,500 mg 3 times/wk or 2,000 mg 2
times/wk; 56–75 KG: 1,500 mg once daily
USES or 2,500 mg 3 times/wk or 3,000 mg 2
Adjunctive treatment of tuberculosis in con- times/wk; 76–90 KG: 2,000 mg once daily
junction with other antitubercular agents. or 3,000 mg 3 times/wk or 4,000 mg 2
times/wk (maximum dose regardless of
weight). CHILDREN: 30–40 mg/kg/dose
PRECAUTIONS once daily. Maximum: 2,000 mg/day.
Contraindications: Hypersensitivity to
pyrazinamide. Acute gout, severe hepatic Dosage in Renal/Hepatic Impairment
dysfunction. Cautions: Diabetes, por- CrCl less than 30 mL/min or receiv-
phyria, renal impairment, history of gout, ing HD: 25–35 mg/kg/dose 3 times/wk
history of alcoholism, concurrent medi- (give after dialysis). Contraindicated in
cation associated with hepatotoxicity. severe hepatic impairment.
ACTION SIDE EFFECTS
Exact mechanism unknown. May disrupt Frequent: Arthralgia, myalgia (usually
Mycobacterium tuberculosis membrane mild, self-limited). Rare: Hypersensitiv-
transport. Therapeutic Effect: Bacte- ity reaction (rash, pruritus, urticaria),
riostatic or bactericidal, depending on photosensitivity, gouty arthritis.
underlined – top prescribed drug
pyridostigmine 981

ADVERSE EFFECTS/TOXIC uCLASSIFICATION


REACTIONS PHARMACOTHERAPEUTIC: Anticho-
Hepatotoxicity, gouty arthritis, thrombo- linesterase inhibitor. CLINICAL: Cho-
cytopenia, anemia occur rarely. linergic muscle stimulant.
NURSING CONSIDERATIONS
USES
BASELINE ASSESSMENT Treatment of myasthenia gravis.
Question for hypersensitivity to pyrazin-
amide, isoniazid, ethionamide, niacin. PRECAUTIONS
Ensure collection of specimens for cul- Contraindications: Hypersensitivity to
ture, sensitivity. Obtain CBC, LFT, serum pyridostigmine. Mechanical, intestinal
uric acid levels. or urinary obstruction. Cautions: Bron-
chial asthma, COPD, bradycardia, sei-
INTERVENTION/EVALUATION
zure disorder, hyperthyroidism, cardiac
Monitor LFT results; be alert for hepatic arrhythmias, peptic ulcer, renal impair-
reactions: jaundice, malaise, fever, ab- ment.
dominal (RUQ) tenderness, anorexia,
nausea, vomiting (stop drug, notify phy- ACTION
sician promptly). Check serum uric acid Prevents destruction of acetylcholine
levels; assess for hot, painful, swollen by inhibiting the enzyme acetylcholin-
joints, esp. big toe, ankle, knee (gout). esterase, enhancing impulse transmis-
Evaluate serum blood glucose levels, sion across neuromuscular junction.
diabetic status carefully (pyrazinamide Therapeutic Effect: Produces miosis;
makes management difficult). Assess for increases intestinal, skeletal muscle tone;
rash, skin eruptions. Monitor CBC for stimulates salivary, sweat gland secretions.
thrombocytopenia, anemia.
PHARMACOKINETICS P
PATIENT/FAMILY TEACHING
Poorly absorbed from GI tract. Metabo-
• Do not skip doses; complete full lized in liver. Excreted primarily un-
length of therapy (may be mos or changed in urine. Half-life: 1–2 hrs.
yrs). • Office visits, lab tests are essen-
tial part of treatment. • Take with food LIFESPAN CONSIDERATIONS
to reduce GI upset. • Avoid excessive Pregnancy/Lactation: Unknown if
exposure to sun, ultraviolet light until drug crosses placenta or is distributed
photosensitivity is determined. • Re- in breast milk. Children: Safety and ef-
port any new symptom, immediately for ficacy not established. Elderly: No age-
jaundice (yellowing sclera of eyes/skin); related precautions noted.
unusual fatigue; fever; loss of appetite;
hot, painful, swollen joints. INTERACTIONS
DRUG: None significant. HERBAL: None
significant. FOOD: None known. LAB
pyridostigmine VALUES: None significant.

AVAILABILITY (Rx)
peer-id-oh-stig-meen Injection Solution: (Regonol): 5 mg/mL.
(Mestinon, Mestinon SR , Regonol) Syrup: (Mestinon): 60 mg/5 mL. Tablets:
Do not confuse pyridostigmine (Mestinon): 60 mg.
with physostigmine, or Regonol
with Reglan or Renagel. Tablets: Extended-Release: (Mesti-
non Timespan): 180 mg.

Canadian trade name Non-Crushable Drug High Alert drug


982 pyridostigmine

ADMINISTRATION/HANDLING dia, short periods of atrial fibrillation


IV, IM (in hyperthyroid pts), marked drop in
• Give large parenteral doses concur- B/P (in hypertensive pts).
rently with 0.6–1.2 mg atropine sulfate
IV to minimize side effects. ADVERSE EFFECTS/TOXIC
PO
REACTIONS
• Give with food, milk. • Tablets may be Overdose may produce cholinergic cri-
crushed. Do not chew, crush extended- sis, manifested as increasingly severe
release tablets (may be broken). • Give descending muscle weakness (appears
larger dose at times of increased fatigue first in muscles involving chewing, swal-
(e.g., for those with difficulty in chewing, lowing, followed by muscle weakness
30–45 min before meals). of shoulder girdle, upper extremities),
respiratory muscle paralysis, followed
IV INCOMPATIBILITIES by pelvis girdle/leg muscle paralysis.
Do not mix with any other medications. Requires withdrawal of all cholinergic
drugs and immediate use of 1–4 mg atro-
INDICATIONS/ROUTES/DOSAGE pine sulfate IV for adults, 0.01 mg/kg for
Note: Highly individualized dosing infants and children younger than 12 yrs.
ranges. NURSING CONSIDERATIONS
Myasthenia Gravis BASELINE ASSESSMENT
PO: ADULTS, ELDERLY: (Immediate-Re- Larger doses should be given at time of
lease): Initially, 60 mg 3 times/day. Dos- greatest fatigue. Assess muscle strength
age increased at 48-hr intervals. Main- before testing for diagnosis of myasthenia
tenance: 60 mg–1.5 g/day divided into gravis and following drug administration.
5–6 doses/day. (Usual dose: 600 mg/day.) Avoid large doses in pts with megacolon,
P CHILDREN: Initially, 1 mg/kg/dose q4–6h.
reduced GI motility.
Maximum: 7 mg/kg/24 hr divided into
5–6 doses. Usual dose: 600 mg/day. INTERVENTION/EVALUATION
PO: (Extended-Release): ADULTS, EL- Have facial tissues readily available at pt’s
DERLY: 180–540 mg 1–2 times/day with bedside. Monitor respirations closely dur-
at least a 6-hr interval between doses. ing myasthenia gravis testing or if dosage is
IV, IM: ADULTS, ELDERLY: 2 mg or 1/30th of increased. Assess diligently for cholinergic
oral dose q2–3h. CHILDREN: 0.05–0.15 mg/ reaction, bradycardia in myasthenic pt in
kg/dose. Maximum single dose: 10 mg. crisis. Coordinate dosage time with peri-
ods of fatigue and increased/decreased
Dosage in Renal/Hepatic Impairment muscle strength. Monitor for therapeutic
No dose adjustment. response to medication (increased mus-
cle strength, decreased fatigue, improved
SIDE EFFECTS chewing/swallowing functions).
Frequent: Miosis, increased GI/skeletal
muscle tone, bradycardia, constriction PATIENT/FAMILY TEACHING
of bronchi/ureters, diaphoresis, in- • Report nausea, vomiting, diarrhea,
creased salivation. Occasional: Head- diaphoresis, profuse salivary secretions,
ache, rash, temporary decrease in palpitations, muscle weakness, severe
­diastolic B/P with mild reflex tachycar- abdominal pain, difficulty breathing.

underlined – top prescribed drug


QUEtiapine 983
glaucoma, diabetes, visual problems, el-
QUEtiapine derly, pts at risk for orthostatic hypoten-
sion. Avoid use in pts at risk for torsades de
kwet-eye-a-peen pointes (hypokalemia, hypomagnesemia,
(SEROquel, SEROquel XR) history of cardiac arrhythmias, congenital
j BLACK BOX ALERT jIncreased long QT syndrome, concurrent medications
risk of suicidal ideation and behav- that prolong QT interval).
ior in children, adolescents, young
adults 18–24 yrs with major depres- ACTION
sive disorder, other psychiatric
disorders. Elderly with dementia- Antagonizes DOPamine and serotonin
related psychosis are at increased (antipsychotic activity), histamine (som-
risk for death. nolence), alpha1-adrenergic (orthostatic
Do not confuse QUEtiapine with hypotension) receptors. Therapeutic
OLANZapine, or SEROquel with Effect: Diminishes symptoms associated
SINEquan. with schizophrenia/bipolar disorders.
uCLASSIFICATION PHARMACOKINETICS
PHARMACOTHERAPEUTIC: Dibenzo- Rapidly absorbed. Protein binding: 83%.
diazepine derivative. CLINICAL: Sec- Widely distributed in tissues; CNS con-
ond-generation (atypical) antipsy- centration exceeds plasma concentration.
chotic. Metabolized in liver. Primarily excreted in
urine. Half-life: 6 hrs.
USES LIFESPAN CONSIDERATIONS
Treatment of schizophrenia. Treatment Pregnancy/Lactation: Unknown if drug
of acute manic episodes associated with is distributed in breast milk. Not recom-
bipolar disorder (alone or in combina- mended for breastfeeding mothers. Chil-
tion with lithium or valproate). Mainte- dren: Safety and efficacy not established
nance treatment of bipolar disorder as an in children less than 10 yrs of age (bipolar
­adjunct to lithium or valproic acid. Treat- mania) or less than 13 yrs of age (schizo- Q
ment of acute depressive episodes asso- phrenia). Elderly: No age-related precau-
ciated with bipolar disorder. Extended- tions noted, but lower initial and target dos-
Release Only: Adjunctive treatment ages may be necessary.
to antidepressants in major depressive
disorder (MDD). OFF-LABEL: Delirium INTERACTIONS
in critically ill pts, psychosis/agitation re- DRUG: Medications prolonging QT
lated to Alzheimer’s dementia. Treatment interval (e.g., amiodarone, cital-
of autism, treatment-resistant obsessive opram, dasatinib, haloperidol,
compulsive disorder. ondansetron) may increase risk of
QT prolongation. Alcohol, other CNS
PRECAUTIONS depressants (e.g., LORazepam,
Contraindications: Hypersensitivity to QUE- morphine, zolpidem) may increase
tiapine. Cautions: Renal / hepatic impair- CNS depression. May increase hypo-
ment, preexisting abnormal lipid profile, pts tensive effects of antihypertensives.
at risk for aspiration pneumonia, cardiovas- Strong CYP3A4 inducers (e.g., car-
cular disease (e.g., HF, history of MI), cere- BAMazepine, phenytoin, rifAMPin)
brovascular disease, dehydration, hypovo- may decrease concentration/effect.
lemia, history of drug abuse/dependence, Strong CYP3A4 inhibitors (e.g.,
seizure disorder, hypothyroidism, pts at risk clarithromycin, ketoconazole)
for suicide, Parkinson’s disease, decreased may increase concentration/effect.
GI motility, urinary retention, narrow-angle Anticholinergic agents (e.g., acli-

Canadian trade name Non-Crushable Drug High Alert drug


984 QUEtiapine
dinium, ipratropium, tiotropium, (Extended-Release): Initially, 300 mg/
umeclidinium) may increase anticho- day. May increase in increments of up to
linergic effect. HERBAL: Herbals with 300 mg/day at intervals as short as 1 day.
sedative properties (e.g., chamo- Range: 400–800 mg/day. Maximum: 800
mile, kava kava, valerian) may mg/day. (Immediate-Release): CHILDREN
increase CNS depression. St. John’s 13 YRS AND OLDER: Initially, 25 mg twice
wort may decrease concentration/ daily on day 1, 50 mg twice daily on day 2,
effect. FOOD: None known. LAB VAL- then increase by 100 mg/day to target dose
UES: May decrease total free thyroxine of 400 mg twice daily on day 5. May further
(T4) serum levels. May increase serum increase to 800 mg/day in increments of
cholesterol, triglycerides, ALT, AST, 100 mg or less daily. Range: 400–800 mg/
WBC, GGT. May produce false-positive day. Maximum: 800 mg. Total dose may
pregnancy test result. be divided in 3 doses/day. (Extended-Re-
lease): Initially, 50 mg once daily on day 1,
AVAILABILITY (Rx) 100 mg on day 2, until 400 mg once daily is
Tablets:25 mg, 50 mg, 100 mg, 200 reached on day 5. Range: 400–800 mg/day.
mg, 300 mg, 400 mg. Tablets, Extended- Maximum: 800 mg/day.
Release: 50 mg, 150 mg, 200 mg, 300
mg, 400 mg. Mania in Bipolar Disorder
PO: (Immediate-Release): ADULTS,
ADMINISTRATION/HANDLING ELDERLY: Initially, 100-200 mg once daily
PO at bedtime or in 2 divided doses on day 1.
• Give immediate-release tablets without May increase in increments of 100 mg/day
regard to food. • Do not break, crush, to 200 mg twice daily on day 4. May further
dissolve, or divide extended-release tab- increase in increments of 200 mg/day to
lets. • Extended-release tablets should 800 mg/day Maximum: 800 mg/day. (Ex-
be given without regard to food or with a tended-Release): Initially, 300 mg on day
light meal in evening. 1 in the evening; increase to 600 mg on day
2 . Adjust dose base on response/tolerabil-
Q INDICATIONS/ROUTES/DOSAGE ity. Maximum: 800 mg/day. (Immediate-
• When restarting pts who have been off Release): CHILDREN 10 YRS AND OLDER: 25
QUEtiapine for less than 1 wk, titration mg twice daily on day 1, 50 mg twice daily
is not required and maintenance dose on day 2, then 100 mg twice daily on day
can be reinstituted. • When resta­rting 3, 150 mg twice daily on day 4, then con-
pts who have been off QUEtiapine for tinue at target dose of 200 mg twice daily on
longer than 1 wk, follow initial titration day 5. Usual range: 200-300mg twice daily.
schedule. • When discontinuing, gradual Maximum: 600 mg/day. (Extended-
tapering recommended to avoid withdrawal Release): 50 mg on day 1; 100 mg on day
symptoms and minimize risk of relapse. 2; then increase by 100 mg/day until target
dose of 400 mg once daily on day 5. Usual
Schizophrenia range: 400–600 mg once daily.
PO: (Immediate-Release): ADULTS,
ELDERLY: Initially, 25 mg twice daily, then Depression in Bipolar Disorder
increase in 25–50-mg increments divided PO: (Immediate-Release): ADULTS,
2–3 times/day on the second and third days; ELDERLY: Initially, 50 mg/day on day 1, in-
may further increase up to target dose of crease to 100 mg/day on day 2, then
300–400 mg/day in 2–3 divided doses by increase by 50–100 mg/day up to target
the fourth day. Further adjustments of 25– dose of 300 mg/day. (Extended-Re-
50 mg twice daily may be made at intervals lease): Initially, 50 mg on day 1 in the
of 2 days or longer. Maintenance: 400- evening, 100 mg on day 2, 200 mg on day
800 mg/day. Maximum: 800 mg/day. 3, 300 mg on day 4 and thereafter.

underlined – top prescribed drug


quinapril 985
Adjunctive Therapy in MDD
of bowel activity, stool consistency. As-
PO: ADULTS, ELDERLY: (Extended-
sess for therapeutic response (improved
Release): Initially, 50 mg on days 1 and
thought content, increased ability to con-
2; then 150 mg on days 3 and 4; then centrate, improvement in self-care). Eye
150–300 mg/day thereafter. exam to detect cataract formation should
Dosage in Hepatic Impairment be obtained q6mos during treatment.
(Immediate-Release): Initially, 25 mg/ PATIENT/ FAMILY TEACHING
day. Increase by 25–50 mg/day to effec- • Avoid exposure to extreme heat.
tive dose. (Extended-Release): Initially, • Drink fluids often, esp. during physical
50 mg/day, increase by 50 mg/day until ef- activity. • Take medication as ordered;
fective dose. do not stop taking or increase dos-
Dosage in Renal Impairment age. • Drowsiness generally subsides
No dose adjustment. during continued therapy. • Avoid tasks
that require alertness, motor skills until
SIDE EFFECTS response to drug is established. • Avoid
Frequent (19%–10%): Headache, drowsi- alcohol. • Slowly go from lying to stand-
ness, dizziness. Occasional (9%–3%): Con- ing. • Report suicidal ideation, unusual
stipation, orthostatic hypotension, tachy­ changes in behavior.
cardia, dry mouth, dyspepsia, rash,
asthenia, abdominal pain, rhinitis. Rare
(2%): Back pain, fever, weight gain.
quinapril
ADVERSE EFFECTS/TOXIC
REACTIONS kwin-a-pril
Overdose may produce heart block, hy- (Accupril)
potension, hypokalemia, tachycardia. j BLACK BOX ALERT jMay
cause fetal injury, mortality. Dis-
NURSING CONSIDERATIONS continue as soon as possible once
pregnancy detected. Q
BASELINE ASSESSMENT Do not confuse Accupril with
Assess behavior, appearance, emotional Accolate, Accutane, Aciphex, or
status, response to environment, speech Monopril.
pattern, thought content. Obtain baseline FIXED-COMBINATION(S)
CBC, hepatic enzyme levels before initi-
ating treatment and periodically thereaf- Accuretic: quinapril/hydroCHLORO-
ter. Question medical history as listed in thiazide (a diuretic): 10 mg/12.5 mg,
­Precautions. 20 mg/12.5 mg, 20 mg/25 mg.
INTERVENTION/EVALUATION uCLASSIFICATION
Monitor mental status, onset of extrapyra- PHARMACOTHERAPEUTIC: Angio-
midal symptoms. Assist with ambulation tensin-converting enzyme (ACE) in-
if dizziness occurs. Supervise suicidal- hibitor. CLINICAL: Antihypertensive.
risk pt closely during early therapy (as
psychosis, depression lessens, energy
level improves, increasing suicide poten- USES
tial). Monitor B/P for hypotension, lipid Treatment of hypertension. Used alone or
profile, blood glucose, CBC, or worsen- in combination with other antihyperten-
ing depression, unusual behavior. Assess sives. Adjunctive therapy in management
pulse for tachycardia (esp. with rapid in- of HF. OFF-LABEL: Treatment of pediatric
crease in dosage). Monitor daily pattern hypertension.

Canadian trade name Non-Crushable Drug High Alert drug


986 quinapril

PRECAUTIONS (e.g., losartan, valsartan) may in-


Contraindications: Hypersensitivity to quin­ crease adverse effects. May increase
april. History of angioedema from previous adverse effects of lithium, sacubi-
treatment with ACE inhibitors, concomi- tril. HERBAL: Herbals with hyper-
tant use with aliskiren in pts with diabetes. tensive properties (e.g., licorice,
Concomitant use with neprilysin inhibitor yohimbe) or hypotensive proper-
(e.g., sacubitril) or within 36 hrs of switch- ties (e.g., garlic, ginger, ginkgo
ing to or from neprilysin inhibitor. Cau- biloba) may alter effects. FOOD: None
tions: Renal impairment, hypertrophic car- known. LAB VALUES: May increase
diomyopathy with outflow tract obstruction, serum BUN, alkaline phosphatase,
major surgery, HF, hypovolemia, unstented bilirubin, creatinine, potassium, ALT,
bilateral renal artery stenosis, hyperkale- AST. May decrease serum sodium. May
mia, concurrent potassium supplements, cause positive antinuclear antibody
severe aortic stenosis, ischemic heart dis- (ANA) titer.
ease, cerebrovascular disease.
AVAILABILITY (Rx)
ACTION Tablets: 5 mg, 10 mg, 20 mg, 40 mg.
Suppresses renin-angiotensin-aldosterone
ADMINISTRATION/HANDLING
system, preventing conversion of angio-
tensin I to angiotensin II, a potent vaso- PO
constrictor. Lower angiotensin II causes • Give without regard to food. • Tab-
an increase in plasma renin activity and lets may be crushed.
decreased aldosterone secretion. Thera-
INDICATIONS/ROUTES/DOSAGE
peutic Effect: Reduces peripheral arte-
rial resistance, B/P. Hypertension
PO: ADULTS: Initially, 10–20 mg/day.
PHARMACOKINETICS May adjust dosage at intervals of at least
Route Onset Peak Duration 2 wks or longer up to 80 mg/day in one
PO 1 hr N/A 24 hrs
or two divided doses. ELDERLY: Initially, 10
Q mg once daily. Titrate to optimal response.
Readily absorbed from GI tract. Protein
binding: 97%. Rapidly hydrolyzed to ac- Adjunct to Manage HF
tive metabolite. Primarily excreted in PO: ADULTS, ELDERLY: Initially, 5 mg
urine. Minimal removal by hemodialysis. twice daily. Titrate at wkly intervals to
Half-life: 1–2 hrs; metabolite, 3 hrs 20–40 mg/day in 2 divided doses. Target
(increased in renal impairment). dose: 20 mg twice daily.

LIFESPAN CONSIDERATIONS Dosage in Renal Impairment


Hypertension
Pregnancy/Lactation: Crosses placenta. Creatinine Clearance Initial Dose
Unknown if distributed in breast milk.
More than 60 mL/min 10 mg
May cause fetal, neonatal mortality or
30–60 mL/min 5 mg
morbidity. Children: Safety and efficacy 10–29 mL/min 2.5 mg
not established. Elderly: May be more
sensitive to hypotensive effects. HF
Creatinine Clearance Initial Dose
INTERACTIONS Greater than 30 mL/min 5 mg
DRUG: Aliskiren may increase hyper- 10–30 mL/min 2.5 mg
kalemic effect. May increase potential
for allergic reactions to allopurinol. Dosage in Hepatic Impairment
Angiotensin receptor blockers No dose adjustment.

underlined – top prescribed drug


quinapril 987

SIDE EFFECTS should be made with first urine of day


Frequent (7%–5%): Headache, dizziness. before beginning therapy and periodi-
Occasional (4%–2%): Fatigue, vomiting, cally thereafter. In pts with renal impair-
nausea, hypotension, chest pain, cough, ment, autoimmune disease, or taking
syncope. Rare (less than 2%): Diarrhea, drugs that affect leukocytes or immune
cough, dyspnea, rash, palpitations, im- response, CBC, differential count should
potence, insomnia, drowsiness, malaise. be performed before beginning therapy
and q2wks for 3 mos, then periodically
ADVERSE EFFECTS/TOXIC thereafter.
REACTIONS INTERVENTION/EVALUATION
Excessive hypotension (“first-dose syn-
Monitor B/ P (if excessive reduction in
cope”) may occur in pts with HF, those
B/P occurs, place pt in supine position
who are severely salt/volume depleted.
with legs slightly elevated), renal func-
Angioedema, hyperkalemia occur rarely.
tion, serum potassium, WBC. Assist with
Agranulocytosis, neutropenia may be
ambulation if dizziness occurs. Question
noted in those with collagen vascular
for evidence of headache. Non-cola car-
disease (scleroderma, systemic lupus
bonated beverage, unsalted crackers, dry
erythematosus), renal impairment. Ne-
toast may relieve nausea.
phrotic syndrome may be noted in those
with history of renal disease. PATIENT/ FAMILY TEACHING
• Go slowly from lying to stand-
NURSING CONSIDERATIONS ing. • Full therapeutic effect may take
BASELINE ASSESSMENT 1–2 wks. • Report any sign of infection
Obtain B/P immediately before each dose (sore throat, fever). • Skipping doses
in addition to regular monitoring (be or voluntarily discontinuing drug may
alert to fluctuations). Renal function tests produce severe rebound hyperten-
should be performed before beginning sion. • Avoid tasks that require alert-
therapy. In pts with prior renal disease, ness, motor skills until response to drug
urine test for protein by dipstick method is established. • Avoid alcohol. Q

Canadian trade name Non-Crushable Drug High Alert drug


988 RABEprazole
as delayed-release tablet. Protein bind-
RABEprazole ing: 96%. Metabolized in liver. Primarily
excreted in urine. Half-life: 1–2 hrs
ra-bep-ra-zole (increased with hepatic impairment).
(Aciphex, Aciphex Sprinkle, Pariet )
Do not confuse Aciphex with LIFESPAN CONSIDERATIONS
Accupril or Aricept, or RABE- Pregnancy/Lactation: Unknown if drug
prazole with ARIPiprazole, crosses placenta or is distributed in breast
lansoprazole, omeprazole, or milk. Children: Safety and efficacy not
raloxifene. established. Elderly: No age-related pre-
uCLASSIFICATION
cautions noted.
PHARMACOTHERAPEUTIC: Proton INTERACTIONS
pump inhibitor. CLINICAL: Gastric DRUG: May decrease concentration/effect
acid inhibitor. of acalabrutinib, cefuroxime, erlo-
tinib, neratinib, pazopanib. Strong
USES CYP2C19 inducers (e.g., FLUoxetine),
strong CYP3A4 inducers (e.g., car-
Short-term treatment (4–8 wks), mainte- BAMazepine, phenytoin, rifAMPin)
nance of erosive or ulcerative gastroesoph- may decrease concentration/effect. May
ageal reflux disease (GERD). Treatment of decrease concentration of ketocon-
daytime/nighttime heartburn, other symp- azole, clopidogrel, atazanavir.
toms of GERD. Short-term treatment (4 wks HERBAL: St. John’s wort may decrease
or less) in healing, symptomatic relief of concentration/effects. FOOD: None
duodenal ulcers. Long-­term treatment of known. LAB VALUES: May increase
pathologic hypersecretory conditions, serum ALT, AST, thyroid-stimulating hor-
including Zollinger-Ellison syndrome. mone (TSH).
Treatment of H. pylori (in combination
with amoxicillin and clarithromycin). AVAILABILITY (Rx)
Sprinkle dose form approved for treatment
of GERD in children 1–11 yrs. OFF-LABEL: Tablets, Delayed-Release: 20 mg.
R Maintenance of healing and prevention of Capsule, Sprinkle: 5 mg, 10 mg.
relapse of duodenal ulcers. Treatment of
NSAID-induced ulcers. ADMINISTRATION/HANDLING
PO
PRECAUTIONS • May give without regard to food; best
Contraindications: Hypersensitivity to RABE- taken after breakfast. • Do not break,
prazole, other proton pump inhibitors (e.g., crush, dissolve, or divide tablet; give whole.
omeprazole). Concurrent use with rilpiv-
irine-containing products. Cautions: Severe Sprinkle
hepatic impairment, osteoporosis. • May give with antacid. • Administer
30 min before a meal. • Open capsule,
ACTION sprinkle on soft food. Take within 15 min
Suppresses gastric acid secretion by of preparation. • Do not chew, crush.
inhibiting H+/K+–ATP pump. Therapeu-
tic Effect: Increases gastric pH, reduc- INDICATIONS/ROUTES/DOSAGE
ing gastric acid production. GERD (Erosive or Ulcerative)
PO: ADULTS, ELDERLY: 20 mg/day for
PHARMACOKINETICS 4–8 wks. If inadequate response, may
Rapidly absorbed from GI tract after repeat for additional 8 wks. Mainte-
passing through stomach relatively intact nance: 20 mg/day.

underlined – top prescribed drug


raloxifene 989
Short-Term Treatment of Symptomatic
nausea, diarrhea, headache occurs. As-
GERD
sess skin for evidence of rash. Observe
PO: ADULTS, ELDERLY, CHILDREN 12 YRS
for evidence of dizziness; utilize appro-
AND OLDER: 20 mg/day for 4 wks. If inad-
priate safety precautions.
equate response, may repeat additional 4
wks. CHILDREN, 1–11 YRS, WEIGHING 15 KG PATIENT/FAMILY TEACHING
OR GREATER: 10 mg once daily. WEIGHING • Swallow tablets whole; do not break,
LESS THAN 15 KG: 5 mg once daily; may chew, dissolve, or divide tablets. • Re-
increase to 10 mg once daily. port headache.
Duodenal Ulcer
PO: ADULTS, ELDERLY: 20 mg/day after
morning meal for 4 wks.
raloxifene
Pathologic Hypersecretory Conditions
PO: ADULTS, ELDERLY: Initially, 60 mg ra-lox-i-feen
once daily. May increase to 60 mg twice (Evista)
daily. j BLACK BOX ALERT jIncreases
risk of deep vein thrombosis, pulmo-
H. Pylori Infection nary embolism. Women with coro-
nary heart disease or pts at risk for
PO: ADULTS, ELDERLY: 20 mg twice daily coronary events are at increased
for 10–14 days (given with various anti- risk for death due to stroke.
biotic regimens). Do not confuse Evista with
AVINza.
Dosage in Renal Impairment
No dose adjustment. uCLASSIFICATION

Dosage in Hepatic Impairment PHARMACOTHERAPEUTIC: Selective


Mild to moderate impairment: No estrogen receptor modulator (SERM).
dose adjustment. Severe impairment: CLINICAL: Osteoporosis preventive.
Use caution.
SIDE EFFECTS USES
Prevention/treatment of osteoporosis in R
Rare (less than 2%): Headache, nausea,
dizziness, rash, diarrhea, malaise. postmenopausal women. Reduces risk of
invasive breast cancer in postmenopausal
ADVERSE EFFECTS/TOXIC women with osteoporosis and postmeno-
REACTIONS pausal women at high risk for invasive
Hyperglycemia, hypokalemia, hypona- breast cancer.
tremia, hyperlipemia occur rarely. May PRECAUTIONS
increase risk of bone fractures, C. difficile-
associated colitis. Contraindications: Hypersensitivity to
raloxifene. Active or history of venous
NURSING CONSIDERATIONS thromboembolic events, such as deep
vein thrombosis (DVT), pulmonary
BASELINE ASSESSMENT embolism, retinal vein thrombosis;
Question history of GI disease, ulcers, women who are or may become pregnant,
GERD. breastfeeding. Cautions: Cardiovas-
cular disease, renal/hepatic impair-
INTERVENTION/EVALUATION
ment, risk for venous thromboembolism,
Evaluate for therapeutic response (relief of unexplained uterine bleeding, elevated
GI symptoms). Question if GI discomfort, triglycerides in response to oral estrogen
therapy.
Canadian trade name Non-Crushable Drug High Alert drug
990 raloxifene

ACTION Dosage in Renal/Hepatic Impairment


Selective estrogen receptor modulator No dose adjustment.
(SERM) that binds to estrogen recep- SIDE EFFECTS
tors, increasing bone mineral den-
sity. Blocks estrogen effects in breast/ Frequent (25%–10%): Hot flashes, flu-like
uterus. Therapeutic Effect: Reduces symptoms, arthralgia, sinusitis. Occa-
sional (9%–5%): Weight gain, nausea,
bone resorption, increases bone min-
eral density, reduces incidence of myalgia, pharyngitis, cough, dyspepsia,
fractures. leg cramps, rash, depression. Rare (4%–
3%): Vaginitis, UTI, peripheral edema,
PHARMACOKINETICS flatulence, vomiting, fever, migraine,
Rapidly absorbed after PO administra- diaphoresis.
tion. Protein binding: 95%. Metabolized ADVERSE EFFECTS/TOXIC
in liver. Excreted primarily in feces. REACTIONS
Unknown if removed by hemodialysis.
Half-life: 27.7–32.5 hrs. Pneumonia, gastroenteritis, chest pain,
vaginal bleeding, breast pain occur rarely.
LIFESPAN CONSIDERATIONS
NURSING CONSIDERATIONS
Pregnancy/Lactation: Unknown if
distributed in breast milk. Contraindi- BASELINE ASSESSMENT
cated in pregnancy, breastfeeding. Chil- Question history of thrombosis (CVA,
dren: Not used in this pt population. DVT, PE). Question for possibility of
Elderly: No age-related precautions pregnancy. Drug should be discontin-
noted. ued 72 hrs before and during prolonged
immobilization (postop recovery, pro-
INTERACTIONS longed bed rest). Therapy may be re-
DRUG: Bile acid sequestrants (e.g., sumed only after pt is fully ambulatory.
cholestyramine) may decrease absorp- Determine serum total, LDL cholesterol
tion/effect. May decrease absorption before therapy and routinely thereafter.
of levothyroxine. HERBAL: None sig-
nificant. FOOD: None known. LAB VAL- INTERVENTION/EVALUATION
R UES: May lower serum total cholesterol, Monitor serum total cholesterol, total cal-
LDL. May decrease platelet count, serum cium, inorganic phosphate, total protein,
inorganic phosphate, albumin, calcium, albumin, bone mineral density, platelet
protein. count. Diligently monitor for CVA (aphasia,
blindness, confusion, paresthesia, hemi-
AVAILABILITY (Rx) paresis, syncope), DVT (arm/leg pain,
Tablets: 60 mg. swelling), pulmonary embolism (chest
pain, dyspnea, hypoxia, tachycardia).
ADMINISTRATION/HANDLING
PATIENT/FAMILY TEACHING
PO
• Give without regard to food. • Avoid prolonged restriction of move-
ment during travel (increased risk of ve-
INDICATIONS/ROUTES/DOSAGE nous thromboembolic events). • Take
Note: Discontinue at least 72 hrs prior supplemental calcium, vitamin D if daily
to and during prolonged immobilization dietary intake is inadequate. • Engage in
(may increase risk for DVT/PE). regular weight-bearing exercise. • Mod-
ify, discontinue habits of cigarette smoking,
Prophylaxis/Treatment of Osteoporosis, alcohol consumption. • Report symp-
Breast Cancer Risk Reduction toms of DVT (swelling, pain, hot feeling in
PO: ADULTS, ELDERLY: 60 mg/day. the arms or legs), lung embolism (difficulty

underlined – top prescribed drug


raltegravir 991

breathing, chest pain, rapid heart rate), INTERACTIONS


stroke (blindness, confusion, difficulty DRUG: Proton pump inhibitors (e.g.,
speaking, one-sided weakness, passing omeprazole, pantoprazole) may
out). increase concentration. Aluminum,
magnesium salts, rifAMPin may
decrease levels/effect. HERBAL: None
significant. FOOD: None known. LAB
raltegravir VALUES: May increase serum glucose,
bilirubin, aminotransferase, alkaline
ral-teg-ra-veer phosphatase, amylase, lipase, creatine
(Isentress) kinase. May decrease lymphocytes, neu-
trophils (ANC), Hgb, platelets.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Integrase AVAILABILITY (Rx)
inhibitor. CLINICAL: Antiretroviral 100 mg. Tablets, Chewable:
Packet, Oral:
(anti-HIV). 25 mg, 100 mg.
Tablets, Film-Coated: 400 mg,
600 mg.
USES
Treatment of HIV-1 infection in adults and ADMINISTRATION/HANDLING
children 4 wks and older and weighing PO
at least 3 kg. Used in combination with • Give without regard to food. • Do
at least two other antiretroviral agents. not break, crush, dissolve, or divide film-
OFF-LABEL: Postexposure prophylaxis for coated tablets. • Chewable tablets may
occupational exposure to HIV. be chewed or taken whole. • Oral
Packet: Mix with 5 mL water to provide
PRECAUTIONS a concentration of 20 mg/mL. Once
Contraindications: Hypersensitivity to mixed, measure dose with oral syringe.
raltegravir. Cautions: Elderly, pts at risk Give within 30 min of mixing.
for creatine kinase (CK) elevations and/
or skeletal muscle abnormalities. INDICATIONS/ROUTES/DOSAGE
R
HIV Infection
ACTION PO: ADULTS, ELDERLY, CHILDREN WEIGH-
Inhibits activity of HIV-1 integrase, an ING 40 KG OR MORE: Treatment naïve:
enzyme that incorporates viral DNA into 400 mg twice daily or 1,200 mg
host cell. Therapeutic Effect: Prevents (2 × 600 mg) once daily. Treatment
integration and replication of viral HIV-1. experienced: 400 mg twice daily. (Dos-
age increased to 800 mg twice daily when
PHARMACOKINETICS given with rifAMPin [treatment naïve or
Variably absorbed following PO admin- experienced]). CHILDREN WEIGHING 25 KG
istration. Protein binding: 83%. Metabo- OR MORE (WHO CAN SWALLOW A TAB-
lized in liver. Excreted in feces (51%), LET): 400 mg twice daily. CHILDREN 2–11
urine (32%). Half-life: 9 hrs. YRS WEIGHING 40 KG OR MORE (CHEWABLE
TABLETS): 300 mg twice daily. WEIGH-
LIFESPAN CONSIDERATIONS ING 28–39 KG: 200 mg twice daily. WEIGH-
Pregnancy/Lactation: May cross ING 20–27 KG: 150 mg twice daily.
placenta. Breastfeeding not recom- WEIGHING 14–19 KG: 100 mg twice daily.
mended. Children: Safety and efficacy WEIGHING 11–13 KG: 75 mg twice
not established in pts younger than 4 wks. daily. CHILDREN WEIGHING 14–19 KG (ORAL
Elderly: Age-related hepatic, renal, car- PACKET): 100 mg twice daily. WEIGH-
diac impairment requires strict monitoring. ING 11–13 KG: 80 mg twice daily.
Canadian trade name Non-Crushable Drug High Alert drug
992 ramelteon
WEIGHING 8–10 KG: 60 mg twice daily.
WEIGHING 6–7 KG: 40 mg twice daily. ramelteon
WEIGHING 4–5 KG: 30 mg twice daily.
WEIGHING 3–4 KG: 25 mg twice daily. ra-mel-tee-on
(Rozerem)
Dosage in Renal/Hepatic Impairment Do not confuse ramelteon with
No dose adjustment. Remeron, or Rozerem with
Razadyne or Remeron.
SIDE EFFECTS
Frequent (17%–10%): Diarrhea, nausea, uCLASSIFICATION
headache. Occasional (5%): Fever. Rare PHARMACOTHERAPEUTIC: Melatonin
(2%–1%): Vomiting, abdominal pain, receptor agonist. CLINICAL: Hypnotic.
fatigue, dizziness.
ADVERSE EFFECTS/TOXIC USES
REACTIONS Treatment of insomnia in pts who experi-
Hypersensitivity reactions, anemia, neu- ence difficulty with sleep onset.
tropenia, MI, gastritis, hepatitis, herpes
simplex, toxic nephropathy, renal fail- PRECAUTIONS
ure, chronic renal failure, renal tubular Contraindications: Hypersensitivity to
necrosis occur rarely. ramelteon. Concurrent fluvoxaMINE ther-
apy, history of angioedema with previous
NURSING CONSIDERATIONS ramelteon therapy. Cautions: Depres-
BASELINE ASSESSMENT
sion, other psychiatric conditions, alco-
hol consumption, other CNS depressants,
Obtain baseline CBC, BMP, LFT, CD4 moderate hepatic impairment, severe
count, viral load prior to initiation and sleep apnea, COPD; concomitant strong
at periodic intervals during therapy. Of- CYP1A2 inhibitors (e.g., fluvoxaMINE).
fer emotional support. Obtain medication
history. ACTION
INTERVENTION/EVALUATION Selectively targets melatonin receptors
R Closely monitor for evidence of GI thought to be involved in maintenance
discomfort. Monitor daily pattern of of circadian rhythm underlying nor-
bowel activity, stool consistency. Moni- mal sleep-wake cycle. Therapeutic
tor serum chemistry tests for marked Effect: Prevents insomnia characterized
laboratory abnormalities. Assess for by difficulty with sleep onset.
opportunistic infections: onset of fe- PHARMACOKINETICS
ver, cough, other respiratory symp-
toms. Rapidly absorbed following PO adminis-
tration. Protein binding: 82%. Substantial
PATIENT/FAMILY TEACHING tissue distribution. Metabolized in liver.
• Report fever, abdominal pain, yellow- Excreted in urine (84%), feces (4%).
ing of skin/eyes, dark urine. • Avoid Half-life: 2–5 hrs.
tasks that require alertness, motor skills
until response to drug is estab- LIFESPAN CONSIDERATIONS
lished. • Raltegravir is not a cure for Pregnancy/Lactation: Unknown if
HIV infection, nor does it reduce risk of distributed in breast milk. Breastfeeding
transmission to others. • Pt may con- not recommended. Children: Safety and
tinue to experience illnesses, including efficacy not established. Elderly: Age-
opportunistic infections. related hepatic impairment may require
dosage adjustment.

underlined – top prescribed drug


ramipril 993

INTERACTIONS increased prolactin levels), resulting in


DRUG: Fluconazole, ketoconazole unexplained amenorrhea, galactorrhea,
may increase concentration/effect. CNS decreased libido, impaired fertility. Com-
depressants (e.g., alcohol, morphine, plex sleep-related behavior may occur.
oxyCODONE, zolpidem) may increase
NURSING CONSIDERATIONS
CNS depression. Strong CYP3A4 induc-
ers (e.g., carBAMazepine, rifAMPin) BASELINE ASSESSMENT
may decrease concentration/effect. Fluvox- Assess B/P, pulse, respirations. Raise bed
aMINE may increase concentration/effect; rails, provide call light. Provide environ-
increase risk of toxicity. HERBAL: Herbals ment conducive to sleep (quiet environ-
with sedative properties (e.g., chamo- ment, low/no lighting, TV off).
mile, kava kava, valerian) may increase
CNS depression. FOOD: Onset of action may INTERVENTION/EVALUATION
be reduced if taken with or immediately Assess sleep pattern of pt. Evaluate for
after a high-fat meal. LAB VALUES: May therapeutic response: rapid induction of
decrease serum cortisol. sleep onset, decrease in number of noc-
turnal awakenings.
AVAILABILITY (Rx)
PATIENT/FAMILY TEACHING
Tablets, Film-Coated: (Rozerem): 8 mg.
• Take within 30 min before going to
ADMINISTRATION/HANDLING bed; confine activities to those necessary
PO
to prepare for bed. • Avoid tasks that
• Administer within 30 min before bed- require alertness, motor skills until re-
time. • Do not give with, or immediately sponse to drug is established. • Avoid
following, a high-fat meal. • Do not alcohol. • Do not take medication with
break, crush, dissolve, or divide tablet. or immediately after a high-fat meal.

INDICATIONS/ROUTES/DOSAGE
Insomnia
PO: ADULTS, ELDERLY: 8 mg 30 min ramipril
before bedtime. Maximum: 8 mg. R
ram-i-pril
Dosage in Renal Impairment (Altace)
No dose adjustment. j BLACK BOX ALERT jMay
cause fetal injury, mortality.
Dosage in Hepatic Impairment Discontinue as soon as possible
Mild to moderate impairment: No once pregnancy is detected.
dose adjustment. Severe impairment: Do not confuse Altace with
Not recommended. alteplase, Amaryl, or Artane,
or ramipril with enalapril or
SIDE EFFECTS Monopril.
Frequent (7%–5%): Headache, dizziness, uCLASSIFICATION
drowsiness (expected effect). Occasional
(4%–3%): Fatigue, nausea, exacerbated PHARMACOTHERAPEUTIC: Angio-
insomnia. Rare (2%): Diarrhea, myalgia, tensin-converting enzyme (ACE) in-
depression, altered taste, arthralgia. hibitor. CLINICAL: Antihypertensive.

ADVERSE EFFECTS/TOXIC
REACTIONS USES
May affect reproductive hormones in Treatment of hypertension. Used alone or in
adults (decreased testosterone levels, combination with other antihypertensives.

Canadian trade name Non-Crushable Drug High Alert drug


994 ramipril
Treatment of HF following MI. Reduce risk INTERACTIONS
of heart attack, stroke in pts 55 yrs and DRUG: Aliskiren may increase hyperkale-
older at increased risk of developing major mic effect. May increase potential for aller-
cardiovascular events. OFF-LABEL: HF. Delay gic reactions to allopurinol. Angiotensin
progression of nephropathy, reduce risks of receptor blockers (e.g., losartan, val-
cardiovascular events in hypertensive pts sartan) may increase adverse effects. May
with type 1 or type 2 diabetes. increase adverse effects of lithium, sacu-
bitril. HERBAL: Herbals with hyper-
PRECAUTIONS
tensive properties (e.g., licorice,
Contraindications: Hypersensitivity to yohimbe) or hypotensive properties
ramipril, other ACE inhibitors. His- (e.g., garlic, ginger, ginkgo biloba)
tory of ACE inhibitor–induced angio- may alter effects. FOOD: None known.
edema, concomitant use with aliskiren LAB VALUES: May increase serum BUN,
in pts with diabetes. Concomitant use alkaline phosphatase, bilirubin, creatinine,
or within 36 hrs of switching to or potassium, ALT, AST. May decrease serum
from a neprilysin inhibitor (e.g., sacu- sodium. May cause positive antinuclear
bitril). Cautions: Renal impairment; antibody (ANA) titer.
elderly pts; collagen vascular disease;
hyperkalemia; hypertrophic cardiomy- AVAILABILITY (Rx)
opathy with outflow tract obstruction; Capsules: 1.25 mg, 2.5 mg, 5 mg, 10 mg.
unstented unilateral, bilateral renal
artery stenosis; severe aortic stenosis; ADMINISTRATION/HANDLING
before, during, or immediately after PO
major surgery; concomitant potassium • Give without regard to food. • May
supplements. mix with water, apple juice/sauce.
ACTION INDICATIONS/ROUTES/DOSAGE
Suppresses renin-angiotensin-aldosterone Hypertension (Monotherapy)
system. Blocks conversion of angioten- PO: ADULTS, ELDERLY: Initially, 2.5
sin I to angiotensin II, increases plasma mg/day. Titrate to desired effect after
renin activity, decreases aldoste- 2–4 wks up to 20 mg daily in 1 or 2
R rone secretion. Therapeutic Effect: divided doses. Pts with volume deple-
Reduces peripheral arterial resistance, tion: Initially, 1.25 mg daily. Titrate to
decreasing B/P. desired response.
PHARMACOKINETICS HF Following MI
Route Onset Peak Duration PO: ADULTS, ELDERLY: Initially, 1.25–2.5
PO 1–2 hrs 3–6 hrs 24 hrs mg twice daily. Continue for 1 wk, then
titrate upward q3wks to target dose of 5
Well absorbed from GI tract. Protein mg twice daily.
binding: 73%. Metabolized in liver. Pri-
marily excreted in urine. Not removed by Risk Reduction for MI/Stroke
hemodialysis. Half-life: 5.1 hrs. PO: ADULTS, ELDERLY: Initially, 2.5 mg/day
for 7 days, then 5 mg/day for 21 days, then
LIFESPAN CONSIDERATIONS 10 mg/day as a single dose (or in divided
Pregnancy/Lactation: Crosses placenta. doses in hypertensive or recent post-MI pts).
Distributed in breast milk. May cause
fetal or neonatal mortality or morbidity. Dosage in Renal Impairment
Children: Safety and efficacy not estab- CrCl equal to or less than 40 mL/
lished. Elderly: May be more sensitive min: 25% of normal dose.
to hypotensive effects.

underlined – top prescribed drug


ramucirumab 995
Renal Failure and Hypertension leukocytes or immune response, CBC,
Initially, 1.25 mg/day titrated upward. differential count should be performed
Maximum: 5 mg/day. Renal failure before beginning therapy and q2wks for
and HF: Initially, 1.25 mg/day, titrated 3 mos periodically thereafter. Monitor
up to 2.5 mg twice daily. B/P, renal function, serum potassium,
WBC. Assess for cough (frequent effect).
Dosage in Hepatic Impairment Assist with ambulation if dizziness occurs.
No dose adjustment. Discontinue for Assess lung sounds for rales, wheezing in
jaundice or marked elevation of hepatic pts with HF. Monitor urinalysis for pro-
enzymes. teinuria. Monitor serum potassium in pts
SIDE EFFECTS on concurrent diuretic therapy.
Frequent (12%–5%): Cough, head- PATIENT/FAMILY TEACHING
ache. Occasional (4%–2%): Dizziness, • Do not discontinue medication without
fatigue, nausea, asthenia. Rare (less than physician’s approval. • Slowly go from
2%): Palpitations, insomnia, nervous- lying to standing to minimize hypotensive
ness, malaise, abdominal pain, myalgia. effect. • Report palpitations, cough,
chest pain. • Dizziness may occur in
ADVERSE EFFECTS/TOXIC first few days. • Avoid tasks that require
REACTIONS alertness, motor skills until response to
Excessive hypotension (“first-dose syn- drug is established. • Avoid alco-
cope”) may occur in pts with HF, severely hol. • Report swelling of the face, lips,
salt or volume depleted. Angioedema, or tongue.
hyperkalemia occur rarely. Agranulocyto-
sis, neutropenia may be noted in pts with
collagen vascular disease (scleroderma,
systemic lupus erythematosus), renal ramucirumab
impairment. Nephrotic syndrome may be
noted in those with history of renal dis- ra-mue-sir-ue-mab
ease. May cause angioedema of the face, (Cyramza)
neck, throat, tongue. Cholestatic jaundice, j BLACK BOX ALERT j May
fulminant hepatic necrosis may occur. increase risk of severe, and R
sometimes fatal, hemorrhage, GI
NURSING CONSIDERATIONS hemorrhage, and GI perforation.
Permanently discontinue if severe
BASELINE ASSESSMENT bleeding occurs. May impair wound
Obtain B/P immediately before each healing.
dose, in addition to regular monitoring Do not confuse ramucirumab
(be alert to fluctuations). If excessive with ranibizumab.
reduction in B/P occurs, place pt in su- uCLASSIFICATION
pine position with legs elevated. Renal
function tests should be performed be- PHARMACOTHERAPEUTIC: Vascular
fore beginning therapy. Question history endothelial growth factor (VEGF) inhib-
of hypersensitivity reaction, angioedema. itor. Monoclonal antibody. CLINICAL:
Antineoplastic.
INTERVENTION/EVALUATION
In pts with prior renal disease, urine test
for protein (by dipstick method) should USES
be made with first urine of day before be- As a single agent or in combination with
ginning therapy and periodically thereaf- PACLitaxel, for treatment of advanced or
ter. In pts with renal impairment, autoim- metastatic gastric or gastroesophageal
mune disease, or taking drugs that affect junction adenocarcinoma with disease

Canadian trade name Non-Crushable Drug High Alert drug


996 ramucirumab
progression on or after prior fluoropy- AVAILABILITY (Rx)
rimidine- or platinum-containing chemo- Injection Solution: 100 mg/10 mL, 500
therapy. In combination with DOCEtaxel, mg/50 mL.
for treatment of metastatic non–small-cell
lung cancer (NSCLC) with disease pro- ADMINISTRATION/HANDLING
gression on or after platinum-based che- IV
motherapy. In combination with FOLFIRI,
for treatment of metastatic colorectal • Do not administer IV push or
cancer with disease progression on or bolus. • Recommend premedication
after therapy with bevacizumab, oxalipla- with IV histamine H1 antagonist (e.g.,
tin, and a fluoropyrimidine. Treatment of diphenhydramine) prior to each infusion.
advanced or relapsed/refractory hepato- Pts with prior Grade 1 or Grade 2 infu-
cellular carcinoma (as a single agent). sion reaction should also be premedi-
cated with dexamethasone (or equivalent)
PRECAUTIONS and acetaminophen prior to each infu-
Contraindications: Hypersensitivity to ramu­ sion. • Thoroughly flush IV with 0.9%
cirumab. Cautions: History of arterial/ NaCl upon infusion completion.
venous thromboembolism (e.g., MI, Reconstitution • Calculate dose,
cardiac arrest, CVA, cerebral ischemia), required solution volume, and number of
hepatic cirrhosis, electrolyte imbalance, vials needed using weight in kg. • Vials
hypertension, GI bleeding/perforation, contain either 100 mg/10 mL or 500
chronic/unhealed wounds; baseline neu- mL/50 mL at concentration of 10 mg/mL.
tropenia, thrombocytopenia. • Visually inspect for particulate matter.
Discard if particulate matter or discolor-
ACTION ation observed. • Using 250 mL 0.9%
Binds vascular endothelial growth factor NaCl bag, withdraw and discard a volume
(VEGF) receptor 2 and blocks binding equal to the total calculated volume of
of VEGF ligands, VEGF-A, VEGF-C, and solution. • Slowly add required dose to
VEGF-D. Therapeutic Effect: Inhibits/ diluent bag for final volume of 250 mL.
reduces tumor vascularity and growth. Gently invert bag to mix; do not shake.
Rate of administration • Infuse over
R PHARMACOKINETICS 60 min using 0.22-micron in-line filter
Metabolism not specified. Elimination via dedicated line.
not specified. Storage • Refrigerate vials in original
carton until time of use. • Do not
LIFESPAN CONSIDERATIONS freeze. • Diluted solution may be refriger-
Pregnancy/Lactation: May cause fetal ated up to 24 hrs or stored at room tempera-
harm. Contraception recommended during ture for up to 4 hrs. • Protect from light.
treatment and up to 3 mos after discon-
tinuation. Must either discontinue drug or IV INCOMPATIBILITIES
discontinue breastfeeding. Unknown if dis- Do not dilute in dextrose-containing flu-
tributed in breast milk. Children: Safety ids or infuse concomitantly with other
and efficacy not established. Elderly: No electrolytes or medications.
age-related precautions noted.
INDICATIONS/ROUTES/DOSAGE
INTERACTIONS Gastric Cancer (Advanced or Metastatic)
DRUG: May increase adverse effects/ IV: ADULTS, ELDERLY: 8 mg/kg every 14
toxic reactions of belimumab. HERBAL: days, either as a single agent or in com-
None significant. FOOD: None known. bination with wkly PACLitaxel. Continue
LAB VALUES: May increase urine protein. until disease progression or unaccept-
May decrease neutrophils, serum sodium. able toxicity.
underlined – top prescribed drug
ramucirumab 997
NSCLC SIDE EFFECTS
IV: ADULTS, ELDERLY: 10 mg/kg on day Occasional (16%–9%): Hypertension,
1 of a 21-day cycle in combination with diar­rhea, headache. Ramucirumab
DOCEtaxel. Continue until disease pro- plus Paclitaxel: Frequent (57%–
gression or unacceptable toxicity. 20%): Fatigue, ­diarrhea, peri­pheral
Colorectal Cancer edema, hypertension, stomatitis.
IV: ADULTS, ELDERLY: 8 mg/kg q2wks, in
combination with FOLFIRI (irinotecan, leu- ADVERSE EFFECTS/TOXIC
covorin, 5-fluorouracil). Continue until dis- REACTIONS
ease progression or unacceptable toxicity. Severe, and sometimes fatal, hemorrhagic
Hepatocellular Carcinoma events including GI bleeding occurred in
IV: ADULTS, ELDERLY: 8 mg/kg q2wks (as 3.4% of pts receiving single agent and
single agent). Continue until disease pro- in 4.3% of pts receiving combo therapy.
gression or unacceptable toxicity GI perforations occurred in 0.7% of pts
receiving single agent and in 1.2% of pts
Dose Modification receiving combo therapy. Thromboem-
Based on Common Terminology Criteria bolic events including arterial throm-
for Adverse Events (CTCAE). boembolism, CVA, MI reported in 1.7%
Infusion-related reaction: Reduce of pts. Severe hypertension occurred
infusion rate by 50% for Grade 1 or in 8% of pts receiving single agent and
Grade 2 reaction. Permanently discon- in 15% of pts receiving combo therapy
tinue for Grade 3 or Grade 4 reaction. despite medical management. Severe
Severe hypertension: Interrupt treat- infusion-related reactions such as back
ment until controlled with medical man- pain/spasms, bronchospasm, chest pain,
agement. Permanently discontinue for chills, dyspnea, flushing, hypotension,
severe hypertension that is not controlled hypoxia, paresthesia, rigors/tremors,
with antihypertensive therapy. Protein- supraventricular tachycardia, wheezing
uria: Interrupt treatment for urine pro- occurred in 16% of pts. May cause inef-
tein level greater than or equal to 2 g/24 fective wound healing or wound dehis-
hrs. Restart treatment at reduced dose of cence requiring medical intervention.
6 mg/kg every 14 days once urine protein Reversible posterior leukoencephalopa-
level returns to less than 2 g/24 hrs. If level R
thy syndrome (RPLS) reported in less
greater than or equal 2 g/24 hrs recurs, than 1% of pts. Proteinuria may indicate
interrupt treatment and reduce dose to 5 nephrotic syndrome. Clinical deteriora-
mg/kg every 14 days once level returns to tion of hepatic cirrhosis, manifested by
less than 2 g/24 hrs. Permanently discon- new-onset or worsening ­encephalopathy,
tinue for urine protein level greater than ascites, or hepatorenal syndrome, was
3 g/24 hrs or in the setting of nephrotic reported in pts receiving single agent.
syndrome. Wound healing complica- Other adverse reactions include epi-
tions: Interrupt treatment prior to sched- staxis, intestinal obstruction, neutro-
uled surgery until wound is fully healed. penia, severe rash, thrombocytopenia.
Arterial thromboembolic events, GI Immunogenicity (anti-ramucirumab
perforation, or Grade 3 or Grade 4 antibodies) occurred in 6% of pts.
bleeding: Permanently discontinue.
Dosage in Renal Impairment NURSING CONSIDERATIONS
No dose adjustment.
BASELINE ASSESSMENT
Dosage in Hepatic Impairment Obtain CBC, BMP, urinalysis, urine protein,
Mild to moderate impairment: No vital signs. Assess skin for open wounds.
dose adjustment. Severe impairment: Question possibility of pregnancy,
Use caution.
Canadian trade name Non-Crushable Drug High Alert drug
998 raNITIdine

current breastfeeding status. Receive full Zantac with Xanax, Ziac, Zofran,
medication history including vitamins, or ZyrTEC.
herbal products. Question history of CVA,
hepatic impairment/cirrhosis, hyperten- uCLASSIFICATION
sion, MI, prior hypersensitivity reac- PHARMACOTHERAPEUTIC: Histamine
tion. Offer emotional support. H2-receptor antagonist. CLINICAL: GI
INTERVENTION/EVALUATION agent.
Monitor CBC, electrolytes, urinalysis,
urine protein. Routinely assess vital USES
signs and report hypertension. Persis- Short-term treatment of active duode-
tent diastolic hypertension may indicate nal ulcer. Prevention of duodenal ulcer
hypertensive emergency. Obtain ECG recurrence. Treatment of active benign
for arrhythmia, chest pain, palpitation. gastric ulcer, pathologic GI hypersecre-
Consider RPLS in pts with altered mental tory conditions, acute gastroesophageal
status, confusion, headache, seizure, vi- reflux disease (GERD), including erosive
sual disturbances. Encourage PO intake. esophagitis. Maintenance of healed ero-
Screen for GI bleeding, GI perforation. sive esophagitis. OTC: Relief of heartburn,
Notify physician if any CTCAE toxicities oc- acid indigestion, sour stomach. OFF-
cur (see Appendix M). Monitor for hyper- LABEL: Treatment of upper GI bleeding.
sensitivity reaction. Once infusion is com- Prevention of stress-induced ulcers in ICU.
pleted, IV access must be flushed with NS. Anaphylaxis (adjunct therapy). Premedi-
PATIENT/FAMILY TEACHING cation to prevent taxane hypersensitivity.
• Blood levels will be routinely moni- PRECAUTIONS
tored. • Treatment may cause severe
allergic reaction or infusion-related reac- Contraindications: Hypersensitivity to
tion. • Avoid pregnancy; treatment may raNITIdine. OTC: Do not use if trouble
cause birth defects or miscarriage. Do or pain when swallowing food, vomiting
not breastfeed. Contraception should be with blood, or bloody or black stool is
taken during treatment and up to 3 present. Do not use 150 mg with kidney
mos after discontinuation. • Neurologic disease (unless medically advised). Cau-
R tions: Renal/hepatic impairment, elderly
changes, including altered mental status,
headache, seizures, trouble speaking, pts, history of acute porphyria.
may indicate high blood pressure crisis ACTION
or life-threatening brain swelling. • Im-
mediately report abdominal pain, GI Inhibits histamine action at histamine
bleeding, vomiting blood. • Therapy H2-receptors of gastric parietal cells.
may cause severe blood-clotting events Therapeutic Effect: Inhibits gastric
such as heart attack or stroke. acid secretion. Reduces gastric volume,
hydrogen ion concentration.
PHARMACOKINETICS
raNITIdine Rapidly absorbed from GI tract. Pro-
tein binding: 15%. Widely distributed.
ra-nit-i-deen Metabolized in liver. Primarily excreted
(Apo-RaNITIdine , Zantac, in urine. Not removed by hemodialysis.
Zantac-75, Zantac-150 Maximum Half-life: PO: 2.5 hrs; IV: 2–2.5 hrs
Strength) (increased with renal impairment).
Do not confuse raNITIdine with
amantadine or riMANTAdine, or

underlined – top prescribed drug


raNITIdine 999

LIFESPAN CONSIDERATIONS PO
• Give without regard to food (best given
Pregnancy/Lactation: Unknown if
with meals or at bedtime). • Do not admin-
drug crosses placenta or is distributed in
ister within 1 hr of magnesium- or aluminum-
breast milk. Children: No age-related
containing antacids (decreases absorption).
precautions noted. Elderly: Confusion
more likely with hepatic/renal impairment. IV INCOMPATIBILITIES
INTERACTIONS Amphotericin B complex (Abelcet, AmBi-
some, Amphotec).
DRUG: Magnesium or aluminum antac-
ids may decrease absorption. May decrease IV COMPATIBILITIES
absorption of atazanavir, itraconazole, Dexmedetomidine (Precedex), dilTIAZem
ketoconazole. May decrease concentra- (Cardizem), DOBUTamine (Dobutrex),
tion/effects of acalabrutinib, bosutinib, DOPamine (Intropin), heparin, HYDRO-
cefuroxime, neratinib, pazopanib. May morphone (Dilaudid), insulin, lidocaine,
increase concentration/effect of risedro- LORazepam (Ativan), morphine, norepi-
nate, warfarin. HERBAL: None significant. nephrine (Levophed), potassium chlo-
FOOD: None known. LAB VALUES: Interferes ride, propofol (Diprivan).
with skin tests using allergen extracts. May
increase serum ALT, AST, GGT, creatinine. INDICATIONS/ROUTES/DOSAGE
Duodenal Ulcer
AVAILABILITY (Rx) PO: ADULTS, ELDERLY: Treatment: 150
Capsules: 150 mg, 300 mg. Injection mg twice daily or 300 mg once daily. Mainte-
Solution: 25 mg/mL. Syrup: 15 mg/mL. nance: 150 mg once daily at bedtime. CHIL-
Tablets: 75 mg, 150 mg, 300 mg. DREN 1 MO TO 16 YRS: Treatment: 4–8 mg/
kg/day in 2 divided doses. Maximum: 300
ADMINISTRATION/HANDLING mg/day. Maintenance: 2–4 mg/kg/day
IV once daily. Maximum: 150 mg/day.
Reconstitution • For IV push, dilute Gastric Ulcer (Benign)
each 50 mg with 20 mL 0.9% NaCl, PO: ADULTS, ELDERLY: Treatment: 150
D5W. • For intermittent IV infusion mg 2 times/day. Maintenance: 150 mg
(piggyback), dilute each 50 mg with once daily at bedtime. CHILDREN 1 MO–16 R
0.9% NaCl, D5W to a maximum concen- YRS: Treatment: 4–8 mg/kg/day in 2
tration of 0.5 mg/mL. • For IV infusion, divided doses. Maximum: 300 mg/day.
dilute with 0.9% NaCl, D5W to a maxi- Maintenance: 2–4 mg/kg/day once daily.
mum concentration of 2.5 mg/mL. Maximum (healing): 150 mg/day.
Rate of administration • Administer
Hypersecretory Conditions
IV push over minimum of 5 min (prevents
PO: ADULTS, ELDERLY: 150 mg twice daily
arrhythmias, hypotension). • Infuse IV
up to 6 g/day. IV Infusion: 6.25 mg/hr.
piggyback over 15–20 min. • Infuse IV
infusion over 24 hrs. GERD
Storage • IV solutions appear clear, col- PO: ADULTS, ELDERLY: 75 mg twice daily.
orless to yellow (slight darkening does not If symptoms persist after 2–4 wks, may
affect potency). • IV infusion (piggyback) increase to 150 mg twice daily for 2 wks.
is stable for 48 hrs at room temperature CHILDREN 1 MO TO 16 YRS: 5–10 mg/kg/day
(discard if discolored or precipitate forms). in 2 divided doses. Maximum: 300 mg/day.
IM Erosive Esophagitis
• May be given undiluted. • Give deep PO: ADULTS, ELDERLY: Treatment: 150
IM into large muscle mass. mg 4 times/day. Maintenance: 150 mg
twice daily. CHILDREN 1 MO TO 16
Canadian trade name Non-Crushable Drug High Alert drug
1000 ranolazine
YRS: Treatment: 5–10 mg/kg/day in 2 within 1 hr of magnesium- or aluminum-
divided doses. Maximum: 300 mg/day. containing antacids. • Transient burning/
pruritus may occur with IV administra-
Prevention of Heartburn (OTC) tion. • Report headache. • Avoid alco-
PO: ADULTS, ELDERLY, CHILDREN 12 YRS hol, aspirin.
AND OLDER: 75–150 mg 30–60 min
before eating or drinking beverages that
cause heartburn. Maximum: 2 doses/
day. Do not use more than 14 days. ranolazine
Usual Parenteral Dosage
ra-noe-la-zeen
IV: ADULTS, ELDERLY: 50 mg q6–8h. CHIL-
(Ranexa)
DREN: 2–4 mg/kg/day in divided doses Do not confuse Ranexa with
q6–8h. Maximum: 50 mg/dose. IV infu- CeleXA.
sion: 6.25 mg/hr.
uCLASSIFICATION
Usual Neonatal Dosage
PO: NEONATES: 2 mg/kg/dose q8h. PHARMACOTHERAPEUTIC: Cardio-
IV: NEONATES: Initially, 1.5 mg/kg/dose, vascular agent. CLINICAL: Antianginal
then 1.5–2 mg/kg/day in divided doses q8h. agent.
IV infusion: NEONATES: Loading dose:
1.5 mg/kg, then 1–2 mg/kg/day (0.04– USES
0.08 mg/kg/hr).
Treatment of chronic angina.
Dosage in Renal Impairment
CrCl less than 50 mL/min: Give 150 PRECAUTIONS
mg PO q24h or 50 mg IV q18–24h. Contraindications: Hypersensitivity to rano­
lazine. Hepatic cirrhosis, concurrent use
Dosage in Hepatic Impairment of strong CYP3A inhibitors (e.g., rifAMPin,
No dose adjustment. carBAMazepine) or CYP3A inducers
(e.g., ketoconazole, itraconazole, fluco-
SIDE EFFECTS nazole, clarithromycin, erythromycin).
R Occasional (2%): Diarrhea. Rare (1%): Cautions: Renal/hepatic impairment.
Constipation, headache (may be severe). Preex­isting QT prolongation, concurrent
use with medications known to prolong QT
ADVERSE EFFECTS/TOXIC interval, pts 75 yrs of age or older, hypoka-
REACTIONS lemia, hypomagnesemia.
Reversible hepatitis, blood dyscrasias
occur rarely. ACTION
Inhibits inward current of sodium
NURSING CONSIDERATIONS channel during cardiac repolariza-
BASELINE ASSESSMENT tion, thereby reducing calcium influx.
Decreased influx of calcium reduces
Obtain history of epigastric/abdominal
ventricular tension, myocardial oxygen
pain.
demand. Does not reduce heart rate, B/P.
INTERVENTION/EVALUATION Therapeutic Effect: Exerts antianginal,
Assess mental status in elderly. Question anti-ischemic effects on cardiac tissue.
present abdominal pain, GI distress.
PHARMACOKINETICS
PATIENT/FAMILY TEACHING Absorption highly variable. Peak plasma
• Smoking decreases effectiveness of concentration: 2–5 hrs. Rapidly,
medication. • Do not take medicine extensively metabolized in intestine, liver.

underlined – top prescribed drug


rasagiline 1001
Protein binding: 62%. Excreted in urine SIDE EFFECTS
(75%), feces (25%). Half-life: 7 hrs. Occasional (6%–4%): Dizziness, head-
ache, constipation, nausea. Rare (2%–
LIFESPAN CONSIDERATIONS
1%): Peripheral edema, abdominal pain,
Pregnancy/Lactation: Unknown if drug dry mouth, vomiting, tinnitus, vertigo,
crosses placenta or is distributed in palpitations.
breast milk. Children: Safety and effi-
cacy not established. Elderly: No age- ADVERSE EFFECTS/TOXIC
related precautions noted. REACTIONS
Overdose manifested as confusion, diplo-
INTERACTIONS
pia, dizziness, paresthesia, syncope.
DRUG: See contraindications. Strong
CYP3A4 inducers (e.g., carBAM- NURSING CONSIDERATIONS
azepine, phenytoin, rifAMPin) may
decrease concentration/effect. Calcium BASELINE ASSESSMENT
channel blockers (e.g., dilTIAZem, Receive full medication history and
verapamil), strong CYP3A4 inhibitors screen for contraindications. Question
(e.g., clarithromycin, ketoconazole) history of hepatic impairment, long QT
may increase concentration/effect. May syndrome. Record onset, type (sharp,
increase concentration/effect of digoxin, dull, squeezing), radiation, location,
simvastatin, tacrolimus. HERBAL: St. intensity, duration of anginal pain, pre-
John’s wort may decrease concentration/ cipitating factors (exertion, emotional
effects. FOOD: Grapefruit products may stress). Obtain baseline ECG.
increase plasma concentration, risk of QT INTERVENTION/EVALUATION
prolongation. LAB VALUES: May slightly
elevate serum BUN, creatinine. Assist with ambulation if dizziness oc-
curs. Give with food if nausea occurs.
AVAILABILITY (Rx) Assess for relief of anginal pain. Monitor
ECG, pulse for irregularities.
Tablets, Extended-Release: 500 mg,
1,000 mg. PATIENT/FAMILY TEACHING
• Avoid grapefruit products. • Do not
ADMINISTRATION/HANDLING chew, crush, dissolve, or divide ex- R
PO tended-release tablets. • Avoid tasks
• May give without regard to food. requiring alertness, motor skills until
• Do not break, crush, dissolve, or response to drug is established.
divide extended-release tablets.
INDICATIONS/ROUTES/DOSAGE
Chronic Angina rasagiline
PO: ADULTS, ELDERLY: Initially, 500 mg
twice daily. May increase to 1,000 mg twice ra-sa-ji-leen
daily, based on clinical response. Dose (Azilect, Apo-Rasagiline )
should not exceed 500 mg twice daily when Do not confuse Azilect with
used concurrently with moderate CYP3A Aricept.
inhibitors (e.g., dilTIAZem, verapamil).
uCLASSIFICATION
Dosage in Renal/Hepatic Impairment
PHARMACOTHERAPEUTIC: MAO
No dose adjustment (discontinue if acute type B inhibitor. CLINICAL: Antipar-
renal failure develops). Contraindicated kinson agent.
in pts with cirrhosis.

Canadian trade name Non-Crushable Drug High Alert drug


1002 rasagiline

USES (e.g., dexfenfluramine, fenflura-


Treatment of signs/symptoms of Parkin- mine, sibutramine), CNS stimulants
son’s disease as initial monotherapy or as (e.g., methylphenidate), cyclo-
adjunct therapy with or without levodopa. benzaprine, dextromethorphan,
meperidine, methadone, mirtazap-
PRECAUTIONS ine, serotonin or norepinephrine
Contraindications: Hypersensitivity to reuptake inhibitors (e.g., cital­
rasagiline. Concurrent use with metha- opram, sertraline, venlafaxine),
done, traMADol, meperidine, MAOIs within tricyclic antidepressants (e.g., ami-
14 days of rasagiline, cycloben­ zaprine, triptyline), venlafaxine may cause
dextromethorphan, or St. John’s wort. serotonin syndrome. May increase risk
Cautions: Hepatic impairment (avoid use of atomoxetine, buPROPion toxic-
in moderate to severe impairment); car- ity. Levodopa may cause hypertensive/
diovascular, cerebrovascular disease, pts hypotensive reaction. HERBAL: Herbals
with hypotension. Avoid foods high in tyra- with hypotensive properties (e.g.,
mine. Do not use within 5 wks of stopping black cohosh, garlic) may increase
FLUoxetine; do not start tricyclic, SSRI, or effect. FOOD: Caffeine, foods/bever-
SNRI within 2 wks of stopping rasagiline. ages containing tyramine may result
History of major psychotic disorder. in hypertensive reaction, hypertensive
crisis. LAB VALUES: May increase serum
ACTION alkaline phosphatase, bilirubin, ALT, AST.
Irreversibly and selectively inhibits May cause leukopenia.
monoamine oxidase type B, an enzyme
AVAILABILITY (Rx)
that plays a major role in catabolism
of DOPamine. Inhibition of DOPamine Tablets: 0.5 mg, 1 mg.
depletion reduces symptomatic motor
ADMINISTRATION/HANDLING
deficits of Parkinson’s disease. Thera-
peutic Effect: Reduces symptoms of PO
Parkinson’s disease, appears to delay • Give without regard to food. • Avoid
disease progression. food, beverages containing tyramine
(e.g., cheese, sour cream, yogurt, pick-
R PHARMACOKINETICS led herring, liver, figs, raisins, bananas,
Rapidly absorbed following PO admin- avocados, soy sauce, broad beans, yeast
istration. Protein binding: 88%–94%. extracts, meat tenderizers, red wine,
Metabolized in liver. Excreted in urine beer), excessive amounts of caffeine
(62%), feces (7%). Half-life: 1.3–3 (e.g., coffee, tea).
hrs.
INDICATIONS/ROUTES/DOSAGE
LIFESPAN CONSIDERATIONS b ALERT c When used in combination
Pregnancy/Lactation: Unknown if dis- with levodopa, dosage reduction of le-
tributed in breast milk. Children: Safety vodopa should be considered.
and efficacy not established. Elderly: No
Parkinson’s Disease
age-related precautions noted.
PO: ADULTS, ELDERLY, MONOTHERAPY,
INTERACTIONS ADJUNCTIVE THERAPY WITHOUT LEVODOPA:
1 mg once daily. ADULTS, ELDERLY,
DRUG: Alcohol may increase adverse
ADJUNCTIVE THERAPY WITH LEVODOPA:
effects. Amphetamines, MAOIs (e.g.,
Initially, 0.5 mg once daily. If thera-
phenelzine, selegiline), sympatho-
peutic response is not achieved,
mimetics (e.g., DOPamine) may
dose may be increased to 1 mg once
cause hypertensive crisis. Anorexiants

underlined – top prescribed drug


rasburicase 1003
daily.ADJUNCTIVE THERAPY WITHOUT PATIENT/FAMILY TEACHING
LEVODOPA: 1 mg once daily. • Orthostatic hypotension may occur
more frequently during initial ther-
Dose Modification apy. • Avoid tasks that require alert-
Concomitant use of CYP1A2 inhibi- ness, motor skills until response to drug
tors, ciprofloxacin: 0.5 mg once daily. is established. • Hallucinations may
Dosage in Hepatic Impairment
occur (more so in the elderly with Par-
Mild impairment: 0.5 mg once daily.
kinson’s disease), typically within first 2
Moderate to severe impairment: Not
wks of therapy. • Avoid foods that con-
recom­mended. tain tyramine (cheese, sour cream,
beer, wine, pickled herring, liver, figs,
Dosage in Renal Impairment raisins, bananas, avocados, soy sauce,
No dose adjustment. yeast extracts, yogurt, papaya, broad
beans, meat tenderizers), excessive
SIDE EFFECTS amounts of caffeine (coffee, tea, choco-
Frequent (14%–12%): Headache, nausea. late), OTC preparations for hay fever,
Occasional (9%–5%): Orthostatic hypoten- colds, weight reduction (may produce
sion, weight loss, dyspepsia, dry mouth, significant rise in B/P). • Do not take
arthralgia, depression, hallucinations, con- any newly prescribed medications un-
stipation. Rare (4%–2%): Fever, vertigo, less approved by prescriber who origi-
ecchymosis, rhinitis, neck pain, arthritis, nally started therapy.
paresthesia.
ADVERSE EFFECTS/TOXIC
REACTIONS rasburicase
Increase in dyskinesia (impaired vol-
untary movement), dystonia (impaired ras-bure-i-kase
muscular tone) occurs in 18% of pts, (Elitek, Fasturtec )
angina occurs in 9%. Gastroenteritis, j BLACK BOX ALERT jSevere
conjunctivitis occur rarely (3% of pts). hypersensitivity reactions including
anaphylaxis reported. May cause
NURSING CONSIDERATIONS severe hemolysis in pts with R
glucose-6-phosphate dehydroge-
BASELINE ASSESSMENT nase (G6PD) deficiency. Screen
pts at high risk for G6PD (African
Obtain baseline LFT, blood pressure. Re- or Mediterranean descent) prior to
ceive full medication history and screen for therapy. Methemoglobinemia has
interactions. Question history of severe he- been reported. Blood samples left
patic impairment, cardiovascular disease. at room temperature may interfere
with uric acid measurements. Must
INTERVENTION/EVALUATION collect blood samples in prechilled
tubes containing heparin and
Give with food if nausea occurs. Monitor immediately immerse in ice water
B/P. Instruct pt to slowly go from lying to bath. Assay plasma samples within
standing to prevent orthostatic hypotension. 4 hrs of collection. Elitek enzymati-
Assess for clinical reversal of symptoms cally degrades uric acid in blood
samples left at room temperature.
(improvement of tremor of head/hands at
rest, mask-like facial expression, shuffling uCLASSIFICATION
gait, muscular rigidity). If hallucinations or
dyskinesia occurs, symptoms may be elimi- PHARMACOTHERAPEUTIC: Urate-
nated if levodopa dosage is reduced. Hal- oxidase enzyme. CLINICAL: Antihy-
lucinations generally are accompanied by peruricemic.
confusion and, to a lesser extent, insomnia.

Canadian trade name Non-Crushable Drug High Alert drug


1004 rasburicase

USES vial with 5 mL of diluent to provide con-


Initial management of uric acid levels in centration of 1.5 mg/mL. • Gently swirl
pts with leukemia, lymphoma, and solid to mix. Do not shake. • Inspect for
tumor malignancies who are receiv- particulate matter or discoloration.
ing chemotherapy expected to result in • Inject calculated dose into appropri-
tumor lysis and subsequent elevation of ate volume of 0.9% NaCl to achieve a final
plasma uric acid. volume of 50 mL.
Rate of administration • Infuse over
PRECAUTIONS 30 min. • Do not use filter during
Contraindications: History of anaphylaxis reconstitution or infusion.
or severe hypersensitivity to rasburicase. Storage • Refrigerate solution until
Prior rasburicase-associated drug reac- time of use. • Discard after 24 hrs fol-
tions including hemolysis, methemo- lowing reconstitution.
globinemia. History of G6PD deficiency.
Cautions: Pts at high risk for G6PD defi-
IV INCOMPATIBILITIES
ciency (e.g., African, Mediterranean, or Do not mix with other IV medications.
Southeast Asian descent).
INDICATIONS/ROUTES/DOSAGE
ACTION Note: Indicated only for a single course
A urate-oxidase enzyme that converts of treatment.
uric acid into allantoin (an inactive
metabolite of uric acid). Does not inhibit Management of Hyperuricemia
formation of uric acid. Therapeutic IV: ADULTS, ELDERLY, CHILDREN: 0.05–
Effect: Decreases uric acid levels. 0.2 mg/kg once daily for 1–7 days.

PHARMACOKINETICS Dosage in Renal/Hepatic Impairment


No dose adjustment.
Half-life: 16–23 hrs.
LIFESPAN CONSIDERATIONS SIDE EFFECTS
Frequent (50%–46%): Vomiting, fever.
Pregnancy/Lactation: Unknown if dis­
Occasional (27%–13%): Nausea, head-
tributed in breast milk. Unknown if crosses
R placenta. May cause fetal harm. Children/ ache, abdominal pain, constipation, diar-
Elderly: No age-related precautions rhea, mucositis, rash.
noted. ADVERSE EFFECTS/TOXIC
INTERACTIONS REACTIONS
DRUG: None significant. HERBAL: None Hypersensitivity reactions occurred in
significant. FOOD: None known. LAB 4.3% of pts including injection irritation,
VALUES: May increase serum bilirubin, peripheral edema, urticaria, pruritus.
ALT. May decrease serum phosphate. Anaphylaxis, hemolysis, methemoglo-
binemia occurred in less than 1%. Pul-
AVAILABILITY (Rx) monary hemorrhage, respiratory failure,
Injection, Powder for Reconstitution: 1.5 supraventricular arrhythmias, ischemic
mg/vial, 7.5 mg/vial. coronary artery disorders, sepsis, abdom-
inal, gastrointestinal infections occurred
ADMINISTRATION/HANDLING in greater than 2% of pts. Clinical tumor
lysis syndrome (TLS), manifested by
IV
hyperuricemia, hyperkalemia, hyper-
Reconstitution • Must use diluent phosphatemia, seizure, increased serum
provided in carton. • Reconstitute 1.5- creatinine, renal failure reported in 3% of
mg vial with 1 mL of diluent or 7.5-mg pts. Anti-rasburicase antibodies reported.

underlined – top prescribed drug


regorafenib 1005

NURSING CONSIDERATIONS irinotecan-based chemotherapy, anti-VEGF


or anti-EGFR therapy. Locally advanced,
BASELINE ASSESSMENT unresectable or metastatic GI stromal
Obtain CBC, BMP, LFT, serum phosphate, tumor previously treated with imatinib
uric acid level; urine pregnancy if ap- and SUNItinib. Treatment of hepatocel-
plicable. Question for history of prior lular carcinoma (HCC) previously treated
hypersensitivity reactions. Assess G6PD with sorafenib.
deficiency risk in potential candidates.
PRECAUTIONS
INTERVENTION/EVALUATION Contraindications: Hypersensitivity to rego-
Offer antiemetics to control nausea, rafenib. Cautions: Mild to moderate hepatic
vomiting. Monitor CBC, BMP, LFT, serum impairment (not recommended with severe
phosphate. If hypersensitivity reaction hepatic impairment), hypertension (not
occurs, stop infusion and immediately recommended with severe or uncontrolled
notify physician. Screen for clinical tu- hypertension), recent surgical/dental pro-
mor lysis syndrome, hemolysis, methe- cedures, chronic open wounds/ulcers,
moglobinemia. Follow strict procedure hemoptysis, concomitant warfarin therapy,
when collecting uric acid levels. Obtain cardiovascular disease, recent MI.
ECG for chest pain/tightness, hyperkale-
mia, dyspnea. Assess skin for rash. ACTION
PATIENT/FAMILY TEACHING
Inhibits tyrosine kinase activity involved
with tumor angiogenesis, oncogenesis,
• Report any allergic reaction, broncho- and maintenance of tumor microenvi-
spasm, chest pain or tightness, cough, ronment. Therapeutic Effect: Inhibits
difficulty breathing, dizziness, fainting, tumor cell growth and metastasis.
rash, or itching.
PHARMACOKINETICS
Readily absorbed following PO admin-
istration. Metabolized in liver. Protein
regorafenib binding: 99.5%. Peak plasma concen-
tration: 4 hrs. Excreted in feces (71%),
re-goe-raf-e-nib urine (19%). Half-life: 28 hrs (Range: R
(Stivarga) 14–58 hrs).
j BLACK BOX ALERT jSevere,
sometimes fatal, hepatotoxicity LIFESPAN CONSIDERATIONS
reported. Monitor hepatic function
prior to and during treatment. Inter- Pregnancy/Lactation: May cause fetal
rupt, reduce, or discontinue therapy harm. Not recommended in nurs-
if hepatotoxicity or hepatocellular ing mothers. Unknown if distributed
necrosis occurs. in breast milk. Contraception recom-
mended during treatment and up to 2
uCLASSIFICATION
mos after discontinuation of therapy.
PHARMACOTHERAPEUTIC: Vascular Children: Safety and efficacy not estab-
endothelial growth factor (VEGF) lished. Elderly: No age-related precau-
inhibitor. Tyrosine kinase inhibitor. tions noted.
CLINICAL: Antineoplastic.
INTERACTIONS
DRUG: Strong CYP3A4 inducers (e.g.,
USES carBAMazepine, phenytoin) may
Treatment of metastatic colorectal can- decrease concentration/effects. Strong
cer in pts who have been previously CYP3A4 inhibitors (e.g., clarithro-
treated with fluoropyrimidine/oxaliplatin/ mycin, ketoconazole) may increase

Canadian trade name Non-Crushable Drug High Alert drug


1006 regorafenib
concentration/effects. HERBAL: St. John’s Dosage in Hepatic Impairment
wort may decrease concentration/effects. Mild to moderate impairment: No
FOOD: Grapefruit products may increase dose adjustment. Severe impairment:
concentration/effects. High-fat meal may Not recommended.
increase absorption/concentration. LAB
VALUES: May decrease lymphocytes, neu- SIDE EFFECTS
trophils, platelets, serum calcium, phos- Frequent (64%–26%): Asthenia/fatigue,
phorus, potassium, sodium. May increase anorexia, diarrhea, mucositis, weight
serum bilirubin, ALT, AST, lipase, amylase, loss, hypertension, dysphonia, general-
INR, urine protein. ized pain, fever, rash. Occasional (10%–
5%): Headache, alopecia, dysgeusia,
AVAILABILITY (Rx) musculoskeletal stiffness, dry mouth.
Tablets: 40 mg. Rare (2% or Less): Tremor, gastric reflux.

ADMINISTRATION/HANDLING ADVERSE EFFECTS/TOXIC


REACTIONS
PO
• Take at same time each day with low- May cause GI perforation, GI fistula for-
fat (less than 30%) breakfast. • Give mation. Hemorrhaging of respiratory, GI,
whole; do not break, crush, dissolve, or genitourinary tracts reported in 21% of
divide tablet. pts. Hypertension (30% of pts) may lead
to hypertensive crisis. May cause ineffective
INDICATIONS/ROUTES/DOSAGE wound healing or wound dehiscence requir-
Metastatic Colorectal Cancer, GI Stromal ing medical intervention. Palmar-plantar
Tumor, Hepatocellular Carcinoma erythrodysesthesia syndrome (PPES), a
PO: ADULTS/ELDERLY: 160 mg once chemotherapy-induced skin condition that
daily for first 21 days of each 28-day presents with redness, swelling, numbness,
cycle. Continue until disease progression skin sloughing of hands, feet (45% of pts).
or unacceptable toxicity. Reversible posterior leukoencephalopathy
syndrome (RPLS) reported in less than 1%
Dosage Modification of pts. May induce cardiac ischemia and/or
Symptomatic Hypertension, Toxic Skin MI. Severe, sometimes fatal, hepatotoxicity
R Reactions, Severe Side Effects (Grades 3–4) including hepatocellular necrosis reported
PO: ADULTS/ELDERLY: Reduce dose to in less than 1%. Various, unspecified infec-
120 mg once daily. If recovery does not tions reported in 31% of pts (most likely
occur within 7 days (despite dose reduc- due to neutropenia).
tion), interrupt treatment for minimum
of 7 days and reassess. If recovery does NURSING CONSIDERATIONS
not occur after interruption, reduce dose BASELINE ASSESSMENT
to 80 mg once daily. Discontinue for any Obtain baseline vital signs, CBC with differ-
of the following: intolerance of 80-mg ential, serum magnesium, phosphate, ion-
dose; serum ALT or AST greater than ized calcium, urinalysis, urine pregnancy,
20 times upper limit of normal (ULN); urine protein, LFT, amylase, lipase, PT/
serum ALT/AST greater than 3 times ULN INR. Assess recent surgical/dental proce-
and bilirubin greater than 2 times ULN; dures. Question possibility of pregnancy,
recurrent serum ALT/AST greater than 5 current breastfeeding status. Obtain full
times ULN despite dose of 120 mg; recov- medication history including herbal prod-
ery failure of Grade 3 or 4 side effects, ucts. Question for history of hyperten-
toxic skin reaction. sion, hepatic impairment, cardiovascular
Dosage in Renal Impairment disease. Assess skin for open/unhealed
No dose adjustment. wounds. Offer emotional support.

underlined – top prescribed drug


reslizumab 1007

INTERVENTION/EVALUATION omalizumab, pembrolizumab,


tocilizumab, or vedolizumab, or
Monitor B/P, CBC, electrolytes, urinaly-
Cinqair with Cinryze, Cinolar,
sis. Monitor LFT q2wks for 2 mos, then
Cinobac, Sinemet, Singulair, or
monthly; or every wk if elevated. Persis-
SINEquan.
tent diastolic hypertension may indicate
hypertensive emergency. Obtain ECG for uCLASSIFICATION
palpitation, chest pain, hypokalemia, hy-
PHARMACOTHERAPEUTIC: Interleu-
perkalemia, hypocalcemia, bradycardia,
kin-5 receptor antagonist. Monoclonal
ventricular arrhythmias. Reverse pos-
antibody. CLINICAL: Antiasthmatic.
terior leukoencephalopathy syndrome
(RPLS) should be considered in pts with
seizure, headache, visual disturbances, USES
altered mental status, malignant hyper- Add-on maintenance treatment of pts with
tension. Assess hydration status. Encour- severe asthma, aged 18 yrs and older, and
age PO intake. Immediately report any with an eosinophil phenotype.
hemorrhaging, bloody stools, hematuria,
abdominal pain, hemoptysis (may indi- PRECAUTIONS
cate GI perforation/fistula formation). Contraindications: Hypersensitivity to
PATIENT/FAMILY TEACHING reslizumab. Cautions: History of helminth
• Blood levels will be routinely moni- (parasite) infection; long-term use of cor-
tored. • Avoid pregnancy. Contracep- ticosteroids. Not indicated for treatment
tion should be practiced during treat- of other eosinophilic conditions; relief of
ment and up to 2 mos after last acute bronchospasm, status asthmaticus,
dose. • Report any yellowing of skin or exercise-induced bronchospasm. History
eyes, abdominal pain, bruising, black/ of anaphylaxis.
tarry stools, dark urine, decreased urine ACTION
output, skin changes. • Report neuro-
logic changes including confusion, sei- Exact mechanism unknown. Inhibits sig-
zures, vision loss, high blood pressure naling of interleukin-5 cytokine, reducing
crisis (may indicate RPLS). • Do not production and survival of eosinophils
take herbal products. • Notify physi- responsible for asthmatic inflammation and R
cian before any planned surgical/dental pathogenesis. Therapeutic Effect: Pre-
procedures. • Do not ingest grapefruit vents inflammatory process. Decreases
products. • Take with low-fat food number of asthma exacerbations.
only. • Drink liquids often if diarrhea PHARMACOKINETICS
occurs (may lead to dehydration).
• Immediately report bleeding of any Widely distributed. Degraded into small
kind. • Swallow tablet whole; do not peptides and amino acids via proteolytic
chew, crush, dissolve, or divide. enzymes. Peak plasma concentration:
reached by end of infusion. Excretion not
specified. Half-life: 24 days.
LIFESPAN CONSIDERATIONS
reslizumab Pregnancy/Lactation: Unknown if dis-
res-li-zoo-mab tributed in breast milk. However, human
(Cinqair) immunoglobulin G (IgG) is present in
Do not confuse reslizumab breast milk and is known to cross placenta.
with certolizumab, daclizumab, Children: Safety and efficacy not estab-
eculizumab, efalizumab, lished. Elderly: No age-related precau-
mepolizumab, natalizumab, tions noted.

Canadian trade name Non-Crushable Drug High Alert drug


1008 reslizumab

INTERACTIONS Dosage in Renal/Hepatic Impairment


DRUG: None known. HERBAL: None sig- Not specified; use caution.
nificant. FOOD: None known. LAB VALUES: SIDE EFFECTS
May increase creatine phosphokinase
(CPK). Rare (3%–1%): Oropharyngeal pain,
myalgia.
AVAILABILITY (Rx)
ADVERSE EFFECTS/
Injection Solution: 100 mg/10 mL (10 TOXIC REACTIONS
mg/mL).
Life-threatening anaphylaxis reported in
ADMINISTRATION/HANDLING less than 1% of pts. Hypersensitivity reac-
tions including bronchospasm, dyspnea,
IV hypoxia, rash, urticaria, vomiting usually
Preparation • Allow vial to warm to occurred during infusion or within 20
room temperature. • Visually inspect mins after completion. Less than 1% of pts
for particulate matter or discoloration. reported at least one malignant neoplasm
Solution should appear clear to slightly within 6 mos of initiation. Unknown if
opalescent, colorless to pale yellow. treatment will influence the immunologic
• Proteinaceous particles may be pres- response to helminth (parasite) infec-
ent. • Air bubbles are expected and tion. Immunogenicity (auto-reslizumab
allowed. • Do not use if solution is antibodies) reported in 5% of pts.
cloudy or discolored or if foreign parti-
cles are observed. • Do not shake. NURSING CONSIDERATIONS
• Withdraw proper dose volume from BASELINE ASSESSMENT
vial and dilute in 50 mL 0.9% NaCl
Obtain serum CPK. Verify presence of eo-
bag. • Gently invert to mix. Do not
sinophil phenotype. Question history of
shake (may cause foaming/precipitate
hypersensitivity reaction. Therapy should
formation). • Infuse via dedicated
be administered in a health care setting
line. • After infusion is complete, flush
by medical professionals who are trained
IV line with 0.9% NaCl.
and prepared to readily manage ana-
Rate of administration • Infuse over
phylaxis. Have anaphylactic medications
R 20–50 mins (depending on total volume
(e.g., antihistamine, bronchodilator, cor-
of infusion), using an in-line, low pro-
ticosteroid, EPINEPHrine, H2 receptor
tein-binding filter (pore size: 0.2
antagonist), intubation kit, supplemental
micron).
oxygen readily available before initia-
Storage • Refrigerate unused vials.
tion. Inhaled or systemic corticosteroids
• Do not freeze. • Diluted solution
should not be suddenly discontinued
may be refrigerated or stored at room
upon initiation. Corticosteroids that are
temperature for up to 16 hrs. • If
not gradually reduced may cause with-
refrigerated, allow diluted solution to
drawal symptoms or unmask conditions
warm to room temperature before
that were originally suppressed with
use. • Protect from light.
corticosteroid therapy. Pts with preexist-
IV INCOMPATIBILITIES ing helminth infection should be treated
prior to initiation.
Do not mix or infuse with other
medications. INTERVENTION/EVALUATION
Obtain serum CPK in pts complaining of
INDICATIONS/ROUTES/DOSAGE myalgia. Diligently observe for hypersen-
Asthma (Severe) sitivity/anaphylactic reaction during infu-
IV: ADULTS, ELDERLY: 3 mg/kg once sion and directly after completion. If ana-
q4wks. phylaxis occurs, discontinue infusion and
underlined – top prescribed drug
ribavirin 1009

provide immediate resuscitation support. Do not confuse ribavirin


Early detection is vital. Assess rate, depth, with riboflavin, rifAMPin, or
rhythm of respirations, oxygen saturation Robaxin.
for therapeutic effectiveness. Assess lungs FIXED-COMBINATION(S)
for wheezing, rales. Obtain pulmonary
function test to assess disease improve- With interferon alfa-2b (Rebetron).
ment. Interrupt or discontinue therapy if Individually packaged.
helminth infection occurs, if worsening uCLASSIFICATION
of asthma-related symptoms occurs (esp.
in pts tapering off corticosteroids). Moni- PHARMACOTHERAPEUTIC: Synthetic
tor for increased use of rescue inhalers; nucleoside. CLINICAL: Antihepaciviral.
may indicate deterioration of asthma.
Monitor for primary malignancies. USES
PATIENT/FAMILY TEACHING Inhalation: Treatment of respiratory
• Treatment may cause life-threatening syncytial virus (RSV) infections (esp. in
anaphylaxis. Immediately report allergic pts with underlying compromising con-
reactions such as difficulty breathing, ditions such as chronic lung disorders,
hives, itching, low blood pressure, rash, congenital heart disease, recent trans-
swelling of the face or tongue, sudden plant recipients). Capsule/tablet/oral
coughing, vomiting, wheezing during infu- solution: Treatment of chronic hepatitis
sion or immediately after infusion. C virus infection in pts with compensated
• Therapy not indicated for relief of acute hepatic disease in combination with
asthma or bronchospasm. • Have a res- other medications.
cue inhaler readily available. • In-
creased use of rescue inhalers may indi- PRECAUTIONS
cate worsening of asthma. • Seek medi- Contraindications: Hypersensitivity to
cal attention if asthma symptoms worsen ribavirin. Inhalation: Women who are
or remain uncontrolled. • Do not stop pregnant or may become pregnant.
corticosteroid therapy unless directed by Oral formulations: Hemoglobinopathies
prescriber. • Treatment may increase (e.g., sickle cell anemia), men whose
risk of new cancers or alter the body’s female partner is pregnant, women of R
immune response to parasite infections. childbearing age who are pregnant or
may become pregnant. Concomitant use
of didanosine. Ribasphere, Rebetol
Only: CrCl less than 50 mL/min. Cau-
ribavirin tions: Inhalation: Pts requiring assisted
ventilation, COPD, asthma. PO: Cardiac
rye-ba-vye-rin or pulmonary disease, elderly pts, history
(Rebetol, Ribasphere, Virazole) of psychiatric disorders, renal impair-
j BLACK BOX ALERT j ment, pts with sarcoidosis, pts with base-
Significant teratogenic/embryo- line risk of severe anemia.
cidal effects. Hemolytic anemia
is significant toxicity, usually ACTION
occurring within 1–2 wks. May Inhibits replication of viral RNA, DNA,
worsen cardiac disease and lead to
fatal or nonfatal MI. Inhalation may influenza virus RNA polymerase activity;
interfere with safe and effective interferes with expression of messenger
assisted ventilation. Monotherapy RNA. Therapeutic Effect: Inhibits viral
not effective for chronic hepatitis C protein synthesis.
virus infection.

Canadian trade name Non-Crushable Drug High Alert drug


1010 ribavirin

PHARMACOKINETICS • Solution appears clear, colorless; is


Readily absorbed. Peak concentrations: stable for 24 hrs at room tempera-
Inhalation: At end of inhalation period. ture. • Discard solution for nebuliza-
Capsules: 3 hrs. Tablets: 2 hrs. Pro- tion after 24 hrs. • Discard if
tein binding: None. Metabolized in liver discolored or cloudy. • Add 50–100
and intracellularly. Primarily excreted in mL Sterile Water for Injection or Inhala-
urine. Half-life: Inhalation: 6.5–11 tion to 6-g vial. • Transfer to a flask,
hrs. Capsules: 298 hr at steady state. serving as reservoir for aerosol genera-
Tablets: 120–170 hrs. tor. • Further dilute to final volume of
300 mL, giving solution concentration of
LIFESPAN CONSIDERATIONS 20 mg/mL. • Use only aerosol genera-
Pregnancy/Lactation: Contraindicated tor available from manufacturer of
in pregnancy. Females and males with drug. • Do not give concomitantly with
female partners of reproductive potential other drug solutions for nebuliza-
must use 2 forms of effective contracep- tion. • Discard reservoir solution when
tion during treatment and for at least 6 fluid levels are low and at least
mos after discontinuation. Unknown q24h. • Only experienced personnel
if excreted in breast milk. Children/ should administer drug.
Elderly: No age-related precautions
INDICATIONS/ROUTES/DOSAGE
noted.
Note: Combination therapy with peg-
INTERACTIONS interferon alone is not recommended in
DRUG: May increase the adverse effects HCV guidelines.
of didanosine. Zidovudine may Chronic Hepatitis C Virus Infection
increase adverse effects. HERBAL: None PO: ADULTS, ELDERLY WEIGHING MORE
significant. FOOD: None known. LAB THAN 75 KG: 1,200 mg daily in 2 divided
VALUES: None significant. doses. WEIGHING 74 KG OR LESS: 1,000 mg
AVAILABILITY (Rx) daily in 2 divided doses. LOW INITIAL DOSE:
600 mg/day. May increase as tolerated.
Capsules: (Rebetol, Ribasphere): 200
mg. Powder for Solution, Nebulization: Dosage in Renal Impairment
R (Virazole): 6 g. Solution, Oral: (Rebetol): Capsules/Oral Solution
40 mg/mL. Tablet: 200 mg. (Riba­ ADULTS: CrCl less than 50 mL/min:
sphere): 200 mg, 400 mg, 600 mg. Contraindicated. CHILDREN: Serum cre-
atinine more than 2 mg/dL: Discon-
ADMINISTRATION/HANDLING tinue treatment.
PO Ribasphere Tablets
• Capsules may be taken without regard ADULTS: CrCl less than 50 mL/min:
to food. • Do not break, crush, or open Not recommended.
capsules. • Use oral solution in children
Dosage in Hepatic Impairment
5 yrs or younger, those 47 kg or less, or
Contraindicated.
those unable to swallow. • Give capsules
with food when combined with peginter- Severe Lower Respiratory Tract Infection
feron alfa-2b. • Tablets should be given Caused by Respiratory Syncytial Virus
with food. (RSV)
Inhalation: CHILDREN, INFANTS: Use with
Inhalation Viratek small-particle aerosol generator at
b ALERT c May be given via nasal or concentration of 20 mg/mL (6 g reconsti-
oral inhalation. tuted with 300 mL Sterile Water for Injec-
tion) over 12–18 hrs/day for 3–7 days.

underlined – top prescribed drug


ribociclib 1011

SIDE EFFECTS
Frequent (greater than 10%): Hemolytic ribociclib
anemia, dizziness, headache, fatigue,
fever, insomnia, irritability, depression, rye-boe-sye-klib
emotional lability, impaired concentration, (Kisqali)
alopecia, rash, pruritus, nausea, anorexia, Do not confuse ribociclib with
dyspepsia, vomiting, decreased hemo- palbociclib or riboflavin.
globin, hemolysis, arthralgia, musculo-
uCLASSIFICATION
skeletal pain, dyspnea, sinusitis, flu-like
symptoms. Occasional (10%–1%): Ner- PHARMACOTHERAPEUTIC: Cyclin-
vousness, altered taste, weakness. dependent kinase inhibitor. CLINICAL:
Antineoplastic.
ADVERSE EFFECTS/
TOXIC REACTIONS
Cardiac arrest, apnea, ventilator depen- USES
dence, bacterial pneumonia, pneumonia, Used in combination with an aroma-
pneumothorax occur rarely. If treatment tase inhibitor as initial endocrine-based
exceeds 7 days, anemia may occur. therapy for treatment of postmenopausal
women with hormone receptor (HR)–
NURSING CONSIDERATIONS positive, human epidermal growth factor
receptor 2 (HER2)–negative advanced
BASELINE ASSESSMENT
or metastatic breast cancer. Treatment of
Obtain sputum specimens before giv- HR-positive, HER2-negative advanced or
ing first dose or at least during first 24 metastatic breast cancer (in combination
hrs of therapy. Assess respiratory status with fulvestrant) in pre-/perimenopausal
for baseline. PO: Obtain CBC with dif- or postmenopausal women as initial
ferential, pretreatment and monthly endocrine-based therapy.
pregnancy test for women of childbear-
ing age. PRECAUTIONS
INTERVENTION/EVALUATION Contraindications: Hypersensitivity to
ribociclib. Cautions: Baseline hemato-
Monitor Hgb, Hct, platelets, LFT, I&O, logic cytopenias (anemia, thrombocy- R
fluid balance carefully. Check hematology topenia, lymphopenia, neutropenia);
reports for anemia due to reticulocytosis electrolyte imbalance (correct abnormal-
when therapy exceeds 7 days. For ven- ity prior to treatment), hepatic impair-
tilator-assisted pts, watch for “rainout” ment, Avoid concomitant use of strong
in tubing and empty frequently; be alert CYP3A inhibitors, strong CYP3A induc-
to impaired ventilation/gas exchange due ers, QTc interval–prolonging medica-
to drug precipitate. Assess skin for rash. tions. Avoid use in pts with or at risk for
Monitor B/P, respirations; assess lung QTc prolongation (e.g., congenital long
sounds. QT syndrome, hypokalemia, hypomag-
PATIENT/FAMILY TEACHING nesemia; uncontrolled, significant car-
• Report immediately any difficulty diac disease including MI, HF, unstable
breathing, itching/swelling/redness of eyes, angina, bradyarrhythmias).
severe abdominal pain, bloody diarrhea, ACTION
unusual bleeding/bruising. • Female pts
should take measures to avoid preg- Blocks retinoblastoma protein phosphoryla-
nancy. • Male pts must use condoms tion and prevents progression through cell
during sexual activity. cycle, resulting in arrest of G1 phase. Ther-
apeutic Effect: Inhibits tumor growth.

Canadian trade name Non-Crushable Drug High Alert drug


1012 ribociclib

PHARMACOKINETICS ADMINISTRATION/HANDLING
Widely distributed. Metabolized exten- PO
sively in liver via CYP3A4. Protein bind- • Give with or without food. • Swallow
ing: 70%. Peak plasma concentration: whole. Do not crush, chew, or split (do not
1–4 hrs. Excreted in feces (69%), urine take broken or cracked tablets). If a dose
(23%). Half-life: 30–55 hrs. is missed or vomiting occurs after admin-
istration, do not give extra dose. Adminis-
LIFESPAN CONSIDERATIONS ter next dose at regularly scheduled time.
Pregnancy/Lactation: Indicated for
postmenopausal women; however, may INDICATIONS/ROUTES/DOSAGE
cause fetal harm/malformations when used Breast Cancer (Advanced or Metastatic)
during pregnancy. Females of reproductive Note: A luteinizing hormone–releas-
potential should use effective contraception ing hormone (LHRH) agonist should
during treatment and for up to 3 wks after be administered to premenopausal and
discontinuation. Unknown if distributed perimenopausal women.
in breast milk. Breastfeeding not recom- PO: ADULTS, ELDERLY: 600 mg once daily
mended during treatment and for up to 3 for 21 days, followed by 7 days off treat-
wks after discontinuation. Children: Safety ment of 28-day cycle. Use in combination
and efficacy not established. Elderly: No with an aromatase inhibitor or fulves-
age-related precautions noted. trant. Continue until disease progression
or unacceptable toxicity.
INTERACTIONS
DRUG: Strong CYP3A inhibitors (e.g., Dose Reduction for Adverse Events
clarithromycin, ketoconazole, rito- Starting dose: 600 mg/day. First
navir) may increase concentration/effect. dose reduction: 400 mg/day. Second
Strong CYP3A inducers (e.g., car- dose reduction: 200 mg/day. Unable
BAMazepine, phenytoin, rifAMPin) to tolerate 200 mg/day: Permanently
may decrease concentration/effect. QT discontinue.
interval–prolonging medications
(e.g., amiodarone, azithromycin, ceri- Dose Modification
tinib, haloperidol, moxifloxacin) may Hepoxicity (During Treatment)
R increase risk of QT interval prolongation, Note: Defined as hepatotoxicity without
torsades de pointes. May increase concen- total bilirubin greater than 2 times upper
tration/effect of aprepitant, bosutinib, limit of normal (ULN). If serum ALT, AST
budesonide, naloxegol, neratinib, elevation greater than 3 times ULN with
olaparib, pimozide. May decrease effect total bilirubin greater than 2 times ULN,
of BCG vaccine. May increase adverse permanently discontinue.
effects/toxicity of natalizumab, pimecro- CTCAE Grade 1 serum ALT, AST ele-
limus, tacrolimus. HERBAL: Echinacea, vation (up to 3 times ULN): No dose
St. John’s wort may decrease concentra- adjustment. CTCAE Grade 2 serum ALT,
tion/effect. FOOD: Grapefruit products, AST elevation (greater than 3–5 times
pomegranate may increase concentration/ ULN) with baseline at less than Grade
effect. LAB VALUES: May increase serum 2: Withhold treatment until recovery to less
ALT, AST, bilirubin. May decrease ANC, Hgb, than or equal to baseline grade, then resume
lymphocytes, leukocytes, neutrophils, plate- at same dose level. If baseline at Grade 2, do
lets; serum potassium, phosphate. not withhold treatment. If Grade 2 serum
ALT, AST elevation recurs, then resume
AVAILABILITY (Rx) at reduced dose level. CTCAE Grade 3
Tablets: 200 mg. Blister Pack: (21 tab- serum ALT, AST elevation (greater
lets, 42 tablets, 63 tablets). than 5–20 times ULN): Withhold

underlined – top prescribed drug


ribociclib 1013
treatment until recovery to less than or Other Toxicities
equal to baseline grade, then resume at Any other CTCAE Grade 1 or 2 tox-
reduced dose level. If Grade 3 serum ALT, icities: No dose adjustment. Any other
AST elevation recurs, permanently dis- CTCAE Grade 3 toxicities: Withhold
continue. CTCAE Grade 4 serum ALT, treatment until resolved to Grade 1 or 0,
AST elevation (Greater than 20 times then resume at same dose level. If Grade
ULN): Permanently discontinue. 3 toxicities recur, resume at reduced
Hematologic dose level. Any other CTCAE Grade
CTCAE Grade 1 or 2 neutropenia 4 toxicities: Permanently discontinue.
(ANC 1000 cells/mm3 to less than Concomitant Use of Strong CYP3A
the lower limit of normal): No dose Inhibitors
adjustment. CTCAE Grade 3 neutrope- Reduce initial dose to 400 mg once daily
nia (ANC 500 to less than 1000 cells/ if strong CYP3A inhibitor cannot be dis-
mm3: Withhold treatment until recovery continued. If CYP3A inhibitor is discon-
to Grade 2 or less, then resume at same tinued, increase ribociclib dose (after at
dose level. If Grade 3 neutropenia recurs, least 5 half-lives of CYP3A inhibitor have
withhold treatment until recovery to elapsed) to the dose used prior to initiat-
Grade 2 or less, then resume at reduced ing strong CYP3A inhibitor.
dose level. CTCAE Grade 3 febrile
neutropenia: Withhold treatment until Dosage in Renal Impairment
recovery to Grade 2 or less, then resume Not specified; use caution.
at reduced dose level. Grade 4 neu- Dosage in Hepatic Impairment
tropenia (ANC less than 500 cells/
Mild impairment: No dose adjust-
mm3): Withhold treatment until recov-
ment. Moderate to severe impair-
ery to Grade 2 or less, then resume at ment: Reduce starting dose to 400 mg
reduced dose level. once daily.
QTc Interval Prolongation
QTc interval prolongation greater SIDE EFFECTS
than 480 msec: Withhold treatment
Frequent (52%–17%): Nausea, fatigue,
until resolved to less than 481 msec, then diarrhea, alopecia, vomiting, constipation,
resume at same dose level. If QTc inter- headache, back pain, decreased appetite,
val prolongation greater than 480 msec R
rash. Occasional (14%–11%): Pruritus,
recurs, withhold treatment until resolved pyrexia, insomnia, dyspnea, stomatitis,
to less than 481 msec, then resume at peripheral edema, abdominal pain.
reduced dose level. QTc interval prolon-
gation greater than 500 msec: With- ADVERSE EFFECTS/
hold treatment if QTc interval prolongation TOXIC REACTIONS
greater than 500 msec on at least two Anemia, leukopenia, lymphopenia, neu-
separate ECGs (within same visit). If QTc tropenia, thrombocytopenia are expected
interval prolongation resolves to less than responses to therapy, but more severe
481 msec after withholding treatment, reactions, including febrile neutropenia,
resume at reduced dose level. QTc inter- may be life threatening. CTCAE Grade 3
val prolongation greater than 500
or 4 neutropenia reported in 60% of pts.
msec (or greater than 60 msec from
Severe hepatotoxicity reported in 10% of
baseline) with torsades de pointes,
pts. QTc interval prolongation, infections
polymorphic ventricular tachycardia,
including UTI may occur.
unexplained syncope, symptoms
of serious arrhythmia: Permanently
discontinue.

Canadian trade name Non-Crushable Drug High Alert drug


1014 rifabutin

NURSING CONSIDERATIONS bruising, confusion, amber or dark-col-


ored urine; right upper abdominal pain,
BASELINE ASSESSMENT yellowing of the skin or eyes; heart arrhyth-
Obtain ANC, CBC, BMP, LFT, serum phos- mias (chest pain, difficulty breathing, palpi-
phate; vital signs, weight. Obtain ECG tations, passing out). • Therapy indicated
(note QTc interval). Initiate treatment for postmenopausal women; however, birth
only in pts with QTc interval less than defects may occur when used during preg-
450 msec. Obtain pregnancy test in fe- nancy. Females of childbearing potential
males of reproductive potential. Question should use effective contraception during
plans of breastfeeding. Question history treatment and for at least 3 wks after final
of cardiac disease, cardiac conduction dose. • Do not breastfeed during treat-
disorders, hepatic impairment. Receive ment and for up to 3 wks after final
full medication history including herbal dose. • Do not ingest grapefruit products,
products and screen for interactions. Seville oranges, starfruit, pomegranate,
Screen for risk of bleeding, QTc interval herbal supplements. • Report planned
prolongation, active infection. Obtain di- surgical/dental procedures. • Immedi-
etary consult. Offer emotional support. ately report bleeding of any kind.
INTERVENTION/EVALUATION
Monitor ANC, CBC for myelosuppression;
LFT for hepatotoxicity q2wks for the first rifabutin
2 cycles, then prior to each subsequent
cycle, then as clinically indicated. Moni- rif-a-bue-tin
tor BMP, serum phosphate for electrolyte (Mycobutin)
imbalance; consider correcting imbal- Do not confuse rifabutin with
ances, esp. hypokalemia, hypomagne- rifAMPin.
semia (due to increased risk of cardiac
arrhythmias, torsades de pointes). Ob- uCLASSIFICATION
tain repeat ECG on day 14 of the first PHARMACOTHERAPEUTIC: Rifamy-
cycle and at the beginning of the second cin derivative. CLINICAL: Antimyco-
cycle, or more frequently if QTc interval bacterial.
R prolongation occurs. Monitor daily pat-
tern of bowel activity, stool consistency.
Assess skin for rash, lesions. Monitor USES
weight, I&O. Prevention of disseminated Mycobacte-
rium avium complex (MAC) disease in
PATIENT/FAMILY TEACHING those with advanced HIV infection. OFF-
• Treatment may depress your immune LABEL: Part of multidrug regimen for
system and reduce your ability to fight infec- treatment of MAC. Alternative to rifAMPin
tion. Report symptoms of infection such as as prophylaxis for latent tuberculosis
body aches, burning with urination, chills, infection, part of multidrug regimen for
cough, fatigue, fever. Avoid those with active treatment of active tuberculosis infection.
infection. • Report symptoms of bone
marrow depression such as bruising, fa- PRECAUTIONS
tigue, fever, shortness of breath, weight loss; Hypersensitivity to rifab-
Contraindications:
bleeding easily, bloody urine or utin, other rifamycins (e.g., rifAMPin).
stool. • Do not take newly prescribed Cautions: Severe renal impairment.
medications unless approved by the pre- Avoid use in renal/hepatic impairment;
scriber who originally started treat- do not give for MAC prophylaxis in pts
ment. • Report liver problems such as with active TB.

underlined – top prescribed drug


rifabutin 1015

ACTION Dosage in Renal Impairment


Inhibits DNA-dependent RNA polymerase. CrCl less than 30 mL/min: Reduce
Therapeutic Effect: Prevents MAC dosage by 50%.
disease. Dosage in Hepatic Impairment
PHARMACOKINETICS No dose adjustment.
Readily absorbed from GI tract. Pro- SIDE EFFECTS
tein binding: 85%. Widely distributed. Frequent (30%): Red-orange or red-brown
Crosses blood-brain barrier. Extensive discoloration of urine, feces, saliva,
intracellular tissue uptake. Metabolized skin, sputum, sweat, tears. Occasional
in liver. Excreted in urine (53%), feces (11%–3%): Rash, nausea, abdominal pain,
(30%). Unknown if removed by hemodi- diarrhea, dyspepsia, belching, headache,
alysis. Half-life: 16–69 hrs. altered taste, uveitis, corneal deposits.
Rare (Less Than 2%): Anorexia, flatulence,
LIFESPAN CONSIDERATIONS
fever, myalgia, vomiting, insomnia.
Pregnancy/Lactation: Unknown if drug
crosses placenta or is distributed in ADVERSE EFFECTS/
breast milk. Children/Elderly: No age- TOXIC REACTIONS
related precautions noted. Hepatitis, anemia, thrombocytopenia,
INTERACTIONS neutropenia occur rarely. May cause uve-
itis, C. difficile–associated diarrhea.
DRUG: May decrease concentration/effect
of atovaquone, mycophenolate, teno- NURSING CONSIDERATIONS
fovir. Strong CYP3A4 inducers (e.g.,
carBAMazepine, phenytoin, rifAMPin) BASELINE ASSESSMENT
may decrease concentration/effect. Vori- Obtain chest X-ray; sputum, blood cultures.
conazole may increase concentration/ Biopsy of suspicious node(s) must be done
effect. May decrease therapeutic effect to rule out active tuberculosis. Obtain base-
of oral contraceptives. HERBAL: St. line CBC, serum hepatic function tests.
John’s wort may decrease concentration/
INTERVENTION/EVALUATION
effect. FOOD: High-fat meals may delay
absorption. LAB VALUES: May increase Monitor serum LFT, platelet count, Hgb, R
serum alkaline phosphatase, ALT, AST. Hct. Avoid IM injections, rectal tempera-
tures, other traumas that may induce
AVAILABILITY (Rx) bleeding. Check temperature; notify
Capsules: 150 mg. physician of flu-like syndrome, rash, GI
intolerance. Monitor bowel pattern, stool
ADMINISTRATION/HANDLING consistency.
PO PATIENT/FAMILY TEACHING
• May take with meals to reduce nau-
• Urine, feces, saliva, sputum, perspira-
sea/vomiting.
tion, tears, skin may be discolored brown-
INDICATIONS/ROUTES/DOSAGE orange. • Soft contact lenses may be
permanently discolored. • Rifabutin
Prevention of MAC (Advanced HIV
may decrease efficacy of oral contracep-
Infection)
tives; nonhormonal methods should be
PO: ADULTS, ELDERLY: 300 mg once
considered. • Avoid crowds, those with
daily or 150 mg twice daily to reduce gas-
infection. • Report flu-like symptoms,
trointestinal upset. CHILDREN, INFANTS: 5
nausea, vomiting, dark urine, unusual
mg/kg once daily. Maximum: 300 mg
bruising/bleeding from any site, any visual
once daily.
disturbances, diarrhea.

Canadian trade name Non-Crushable Drug High Alert drug


1016 rifAMPin
Therapeutic Effect: Bactericidal in
rifAMPin susceptible microorganisms.
rif-am-pin PHARMACOKINETICS
(Rifadin, Rofact ) Well absorbed from GI tract (food delays
Do not confuse Rifadin with Ri- absorption). Protein binding: 80%.
fater or Ritalin, or rifAMPin with Widely distributed. Metabolized in liver.
ribavirin, rifabutin, Rifamate, Primarily eliminated by biliary system.
rifapentine, rifAXIMin, or Ritalin. Not removed by hemodialysis. Half-
life: 3–5 hrs (increased in hepatic
FIXED-COMBINATION(S) impairment).
Rifamate: rifAMPin/isoniazid (an anti­
tubercular): 300 mg/150 mg. Rifater: LIFESPAN CONSIDERATIONS
rifAMPin/isoniazid/pyrazinamide (an Pregnancy/Lactation: Crosses placenta.
antitubercular): 120 mg/50 mg/300 Distributed in breast milk. Children/
mg. Elderly: No age-related precautions
noted.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Rifamycin INTERACTIONS
derivative. CLINICAL: Antitubercular. DRUG: May decrease effects of atova-
quone, dilTIAZem, disopyramine,
edoxaban, esomeprazole, metha-
USES
done, mycophenolate, omeprazole,
In combination with other antitubercu- oral anticoagulants (e.g., apixa-
lar agents for initial treatment, retreat- ban, warfarin), oral contraceptives,
ment of active tuberculosis. Eliminates phenytoin, ranolazine, tacrolimus,
meningococci from nasopharynx of tenofovir, zolpidem. HERBAL: None
asymptomatic carriers. OFF-LABEL: significant. FOOD: Food decreases
Prophylaxis of H. influenzae type B extent of absorption. LAB VALUES: May
infection, Legionella pneumonia, seri- increase serum alkaline phosphatase,
ous infections caused by Staphylococ- bilirubin, uric acid, ALT, AST.
R cus spp. (in combination with other
agents). Treatment of prosthetic joint AVAILABILITY (Rx)
infection. Capsules: 150 mg, 300 mg. Injection,
Powder for Reconstitution: 600 mg.
PRECAUTIONS
Contraindications: Concomitant therapy ADMINISTRATION/HANDLING
with atazanavir, darunavir, fosampre-
navir, saquinavir, ritonavir, tipranavir; IV
hypersensitivity to rifAMPin, other rifa- Reconstitution • Reconstitute 600-mg
mycins. Cautions: Hepatic impairment, vial with 10 mL Sterile Water for Injection
active or treated alcoholism, porphyria. to provide concentration of 60 mg/
Concurrent medications associated with mL. • Withdraw desired dose and fur-
hepatotoxicity. ther dilute with 0.9% NaCl or D5W to
concentration not to exceed 6 mg/mL.
ACTION Rate of administration • For IV infu-
Interferes with bacterial RNA synthesis sion only. Avoid IM, SQ administra-
by binding to DNA-dependent RNA poly- tion. • Avoid extravasation (local
merase, preventing attachment to DNA, irritation, inflammation). • Infuse over
thereby blocking RNA transcription. 30 min to 3 hrs.

underlined – top prescribed drug


rifAMPin 1017
Storage • Reconstituted vial is stable ADVERSE EFFECTS/
for 24 hrs. • Once reconstituted vial is TOXIC REACTIONS
further diluted, it is stable for 4 hrs in Hepatotoxicity (risk is increased when
D5W or 24 hrs in 0.9% NaCl. rifAMPin is taken with isoniazid), hepa-
titis, blood dyscrasias, Stevens-Johnson
PO
syndrome, antibiotic-associated colitis
• Preferably give 1 hr before or 2 hrs
occur rarely.
following meals with 8 oz of water (may
give with food to decrease GI upset; will NURSING CONSIDERATIONS
delay absorption). • For pts unable to
swallow capsules, contents may be mixed BASELINE ASSESSMENT
with applesauce, jelly. • Administer at Obtain CBC, renal function test, LFT. Screen
least 1 hr before antacids, esp. those for concomitant medications known to
containing aluminum. cause hepatotoxicity. Question for hyper-
sensitivity to rifAMPin, rifamycins. Ensure
IV INCOMPATIBILITIES collection of diagnostic specimens.
DilTIAZem (Cardizem).
INTERVENTION/EVALUATION
IV COMPATIBILITIES Assess IV site at least hourly during infu-
D5W if infused within 4 hrs (risk of pre- sion; restart at another site at the first sign
cipitation beyond this time period). of irritation or inflammation. Monitor
LFT, assess for hepatitis: jaundice, an-
INDICATIONS/ROUTES/DOSAGE orexia, nausea, vomiting, fatigue, weak-
Tuberculosis ness (hold rifAMPin, inform physician at
Note: A four-drug regimen (ethambu- once). Report hypersensitivity reactions
tol, isoniazid, pyrazinamide, rifAMPin) is promptly: any type of skin eruption, pru-
preferred for initial, empiric treatment. ritus, flu-like syndrome with high dosage.
PO, IV: ADULTS, ELDERLY: 10 mg/kg/day. Monitor daily pattern of bowel activity,
Maximum: 600 mg/day. CHILDREN: 10– stool consistency (potential for antibiotic-
20 mg/kg/day usually as a single daily associated colitis). Monitor CBC results
dose. Maximum: 600 mg/day. for blood dyscrasias; be alert for infection
(fever, sore throat), unusual bruising/ R
Meningococcal Carrier bleeding, unusual fatigue/weakness.
PO, IV: ADULTS, ELDERLY: 600 mg twice
daily for 2 days. PO only: CHILDREN 1 MO PATIENT/FAMILY TEACHING
AND OLDER: 10 mg/kg/dose q12h for 2 • Preferably take on empty stomach with
days. Maximum: 600 mg/dose. CHIL- 8 oz of water 1 hr before or 2 hrs after
DREN YOUNGER THAN 1 MO: 5 mg/kg/dose meal (with food if GI upset). • Avoid
q12h for 2 days. alcohol. • Do not take any other medi-
cations without consulting physician, in-
Dosage in Renal/Hepatic Impairment cluding antacids; must take rifAMPin at
No dose adjustment. least 1 hr before antacid. • Urine, feces,
sputum, sweat, tears may become red-
SIDE EFFECTS orange; soft contact lenses may be perma-
Frequent: Red-orange or red-brown dis- nently stained. • Report any new symp-
coloration of urine, feces, saliva, skin, tom immediately such as yellow eyes/
sputum, sweat, tears. Occasional (5%– skin, fatigue, weakness, nausea/vomiting,
3%): Hypersensitivity reaction (flushing, sore throat, fever, flu, unusual bruising/
pruritus, rash). Rare (2%–1%): Diarrhea, bleeding. • If taking oral contracep-
dyspepsia, nausea, oral candida (sore tives, check with physician (reliability
mouth, tongue). may be affected).

Canadian trade name Non-Crushable Drug High Alert drug


1018 rifAXIMin
FOOD: None known. LAB VALUES: None
rifAXIMin significant.
rif-ax-i-min AVAILABILITY (Rx)
(Xifaxan, Zaxine ) Tablets: 200 mg, 550 mg.
Do not confuse rifAXIMin with
rifAMPin. ADMINISTRATION/HANDLING
uCLASSIFICATION PO
• Give without regard to food. • Do
PHARMACOTHERAPEUTIC: Anti-infec-
not break, crush, dissolve, or divide film-
tive. CLINICAL: Site-specific antibiotic. coated tablets.

USES INDICATIONS/ROUTES/DOSAGE
Traveler’s Diarrhea
Treatment of traveler’s diarrhea caused
PO: ADULTS, ELDERLY, CHILDREN 12 YRS
by noninvasive strains of E. coli. Reduc-
AND OLDER: 200 mg 3 times/day for 3 days.
tion of risk for recurrence of overt
hepatic encephalopathy. Treatment of Hepatic Encephalopathy
irritable bowel syndrome with diarrhea PO: ADULTS, ELDERLY: 550 mg 2 times/
(IBS-D) in adults. OFF-LABEL: Treatment day or 400 mg 3 times/day.
of hepatic encephalopathy. Treatment of
C. difficile–associated diarrhea. IBS-D
PO: ADULTS, ELDERLY: 550 mg 3 times/
PRECAUTIONS day for 14 days. May repeat up to 2 times
Contraindications: Hypersensitivity to if symptoms recur.
rifAXIMin, other rifamycin antibiotics.
Cautions: Severe hepatic impairment. Dosage in Renal/Hepatic Impairment
No dose adjustment.
ACTION
Inhibits bacterial RNA synthesis by SIDE EFFECTS
binding to bacterial DNA-­
dependent Occasional (11%–5%): Flatulence, head-
R RNA polymerase. Therapeutic ache, abdominal discomfort, rectal tenes-
Effect: Bactericidal. mus, defecation urgency, nausea. Rare
(4%–2%): Constipation, fever, vomiting.
PHARMACOKINETICS
Less than 0.4% absorbed after PO admin- ADVERSE EFFECTS/TOXIC
istration. Primarily excreted in feces. REACTIONS
Half-life: 5.85 hrs. Hypersensitivity reaction, superinfection
occur rarely.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if drug NURSING CONSIDERATIONS
is distributed in breast milk. Children: BASELINE ASSESSMENT
Safety and efficacy not established in pts Check baseline hydration status: skin turgor,
younger than 12 yrs for traveler’s diar- mucous membranes for dryness, urinary
rhea; younger than 18 yrs for IBS-D. status. Assess stool frequency, consistency.
Elderly: No age-related precautions
noted. INTERVENTION/EVALUATION
Encourage adequate fluid intake. As-
INTERACTIONS sess bowel sounds for peristalsis. Moni-
DRUG: May decrease effect of BCG (intra- tor daily pattern of bowel activity, stool
vesical). HERBAL: None significant.

underlined – top prescribed drug


risankizumab-rzaa 1019
consistency. Assess for GI disturbances, pathway. Peak plasma concentration:
blood in stool. 3–14 days. Steady state reached in 16
wks. Half-life: 28 days.
PATIENT/FAMILY TEACHING
• Report if diarrhea worsens or if blood LIFESPAN CONSIDERATIONS
occurs in stool, fever develops within 48 hrs. Pregnancy/Lactation: Unknown if dis-
tributed in breast milk. However, human
immunoglobulin G (IgG) is present in
breast milk and is known to cross the
risankizumab-rzaa placenta. Children: Safety and efficacy
not established. Elderly: No age-related
ris-an-kiz-ue-mab-rzaa precautions noted.
(Skyrizi)
Do not confuse risankizumab INTERACTIONS
with ixekizumab. DRUG: May decrease therapeutic effects/
increase adverse effects of live vaccines.
uCLASSIFICATION
Belimumab, infliximab may increase
PHARMACOTHERAPEUTIC: Interleu- immunosuppressive effect. HERBAL:
kin-23 antagonist. Monoclonal anti- None significant. FOOD: None known. LAB
body. CLINICAL: Antipsoriatic agent. VALUES: None known.

AVAILABILITY (Rx)
USES
Injection Solution, Prefilled Syringe: 75
Treatment of moderate to severe plaque mg/0.83 mL.
psoriasis in adults who are candidates for
systemic therapy or phototherapy. ADMINISTRATION/HANDLING
PRECAUTIONS SQ
Contraindications: Hypersensitivity to Preparation • Remove prefilled
risankizumab. Cautions: Conditions pre- syringe from refrigerator and allow solu-
disposing to infection (e.g., diabetes, tion to warm to room temperature
immunocompromised pts, renal failure, (approx. 15–30 min) with needle cap R
open wounds), prior exposure to tuber- intact. • Visually inspect for particulate
culosis or use in pts who reside or travel matter or discoloration. Solution should
to areas where TB is endemic. Avoid use appear clear to slightly opalescent, color-
during active infection. Concomitant use less to slightly yellow in color. Do not use
of live vaccines not recommended. if solution is cloudy or discolored or if
visible particles are observed.
ACTION Administration • Insert needle sub-
Selectively binds to p19 subunit of inter- cutaneously into outer thigh or abdomen
leukin-23 (IL-23) and inhibits inter- and inject solution. Injections to the
action with IL-23 receptor. IL-23 is a outer arms may only be performed by a
cytokine that is involved in inflammatory healthcare professional. • Do not inject
and immune response. Therapeutic into areas of active skin disease or injury
Effect: Alters biologic immune response; such as sunburns, skin rashes, inflamma-
reduces inflammation of psoriatic tion, skin infections, or active psoria-
lesions. sis. • Rotate injection sites. • Do not
administer IV or intramuscularly. • If a
PHARMACOKINETICS dose is missed, administer as soon as
Widely distributed. Degraded into small possible, then give next dose at regularly
peptides and amino acids via catabolic scheduled time.

Canadian trade name Non-Crushable Drug High Alert drug


1020 risedronate
Storage • Refrigerate prefilled if treatment for latent tuberculosis is
syringes in original carton until time of necessary. Screen for active infection
use. • Protect from light. • Do not or chronic infections. Conduct derma-
shake. • Do not freeze or expose to tologic exam; record characteristics of
heating sources. psoriatic lesions. Assess pt’s willingness
to self-inject medication. Teach proper
INDICATIONS/ROUTES/DOSAGE injection techniques.
Plaque Psoriasis
INTERVENTION/EVALUATION
SQ: ADULTS, ELDERLY: 150 mg (two 75-mg
injections) at wk 0 and wk 4, then Assess skin for improvement of lesions.
q12wks thereafter. Monitor for symptoms of tuberculosis
(cough, fatigue, hemoptysis, nocturnal
Dosage in Renal Impairment sweating, weight loss), including those
Mild to severe impairment: Not speci- who tested negative for latent tubercu-
fied; use caution. losis infection prior to initiating therapy.
Interrupt or discontinue treatment if seri-
Dosage in Hepatic Impairment ous infection, opportunistic infection, or
Mild to severe impairment: Not speci- sepsis occurs.
fied; use caution.
PATIENT/FAMILY TEACHING
SIDE EFFECTS • Treatment may depress your immune
Rare (4%–2%): Headache, tension head- system and reduce your ability to fight
ache, sinus headache, fatigue, asthenia, infection. Report symptoms of infection
injection site reactions (bruising, ery- such as body aches, burning with urina-
thema, extravasation, hematoma, hemor- tion, chills, cough, fatigue, fever; fungal
rhage, infection, inflammation, irritation, infections. Avoid those with active infec-
pain, pruritus, swelling, warmth). tion. • Do not receive live vac-
cines. • Expect frequent tuberculosis
ADVERSE EFFECTS/TOXIC screening. Report symptoms of tubercu-
REACTIONS losis such as cough, fatigue, night sweats,
Upper respiratory tract infections (bac- weight loss, or coughing up
R terial, viral, unspecified) including blood. • Report travel plans to possible
nasopharyngitis, pharyngitis, rhinitis, endemic areas.
sinusitis, tonsillitis reported in 13% of
pts. Tinea infections reported in 1% of
pts. Serious infections including cellu-
litis, herpes zoster, osteomyelitis, sepsis risedronate
occurred in less than 1% of pts. Immu-
nogenicity (auto-risankizumab antibod- ris-ed-roe-nate
ies) reported in 24% of pts. (Actonel, Atelvia)
Do not confuse Actonel with
NURSING CONSIDERATIONS Actos, or risedronate with
BASELINE ASSESSMENT alendronate.
Consider completion of age-appropriate FIXED-COMBINATION(S)
immunizations prior to initiation. Pts Actonel with Calcium: risedronate/
should be evaluated for active tuberculo- calcium: 35 mg/6 × 500 mg.
sis and tested for latent infection prior to
initiation and periodically during therapy. uCLASSIFICATION
Induration of 5 mm or greater with tu- PHARMACOTHERAPEUTIC: Bisphos-
berculin skin testing should be consid- phonate. CLINICAL: Calcium regulator.
ered a positive test result when ­assessing
underlined – top prescribed drug
risedronate 1021

USES famotidine, ranitidine), proton pump


Actonel: Treatment of Paget’s disease of inhibitors (e.g., omeprazole, panto-
bone. Treatment/prevention of osteoporo- prazole) may decrease concentration/effect.
sis in postmenopausal women, glucocorti- HERBAL: None significant. FOOD: None
coid-induced osteoporosis (daily dose 7.5 known. LAB VALUES: None significant.
mg predniSONE or greater). Treatment of
AVAILABILITY (Rx)
osteoporosis in men. Atelvia: Treatment of
osteoporosis in postmenopausal women. Tablets: 5 mg, 30 mg, 35 mg, 150
mg. Tablets, Delayed-Release: 35 mg.
PRECAUTIONS
Contraindications: Hypersensitivity to ADMINISTRATION/HANDLING
risedronate, other bisphosphonates PO
(e.g., alendronate); inability to stand or
sit upright for at least 30 min; abnormali- Actonel: • Administer 30–60 min before
ties of esophagus that delay esophageal any food, drink, other oral medications to
emptying; hypocalcemia. Cautions: GI avoid interference with absorption. • Give
diseases (duodenitis, dysphagia, esopha- on empty stomach with full glass of plain
gitis, gastritis, ulcers [drug may exac- water (not mineral water). • Pt must
erbate these conditions]), severe renal avoid lying down for at least 30 min after
impairment (CrCl less than 30 mL/min). swallowing tablet (assists with delivery to
stomach, reduces risk of esophageal irrita-
ACTION tion). • Give whole; do not break, crush,
Inhibits bone resorption by action on dissolve, or divide tablet. • Atelvia: Take
osteoclasts or osteoclast precursors. in morning immediately following break-
Therapeutic Effect: Osteoporosis: fast with at least 4 oz water. • Remain
Decreases bone resorption (indirectly upright for 30 min after taking dose.
increases bone mineral density). Paget’s INDICATIONS/ROUTES/DOSAGE
Disease: Inhibition of bone resorption
Paget’s Disease
causes a decrease (but more normal
architecture) in bone formation. PO: (Actonel): ADULTS, ELDERLY: 30 mg/
day for 2 mos. Retreatment may occur after
PHARMACOKINETICS 2-mo post-treatment observation period. R
Rapidly absorbed. Bioavailability dec­ Prophylaxis, Treatment of
reased when administered with food. Postmenopausal Osteoporosis
Protein binding: 24%. Not metabolized. PO: (Actonel): ADULTS, ELDERLY: 5 mg/
Excreted unchanged in urine, feces. Not day or 35 mg once wkly or 150 mg once
removed by hemodialysis. Half-life: 1.5 monthly.
hrs (initial); 480 hrs (terminal).
Treatment of Postmenopausal
LIFESPAN CONSIDERATIONS Osteoporosis
Pregnancy/Lactation: Unknown if dis- PO: (Atelvia): ADULTS, ELDERLY: 35 mg
tributed in breast milk. Children: Not once wkly.
indicated for use in this pt population.
Elderly: No age-related precautions noted. Treatment of Male Osteoporosis
PO: (Actonel): ADULTS, ELDERLY: 35
INTERACTIONS mg once wkly.
DRUG: Antacids containing aluminum,
calcium, magnesium; vitamin D may Glucocorticoid-Induced Osteoporosis
decrease absorption (avoid administration PO: (Actonel): ADULTS, ELDERLY: 5 mg/
within 30 min of risedronate). Hista- day.
mine H2 receptor antagonists (e.g.,
Canadian trade name Non-Crushable Drug High Alert drug
1022 risperiDONE
Dosage in Renal Impairment pain when swallowing, chest pain, new/
Not recommended with CrCl less than 30 worsening heartburn. • Consider weight-­
mL/min. bearing exercises; modify behavioral
factors (cigarette smoking, alcohol con-
Dosage in Hepatic Impairment sumption). • Report jaw pain, inca-
No dose adjustment. pacitating bone, joint, or muscle pain.
SIDE EFFECTS
Frequent (30%): Arthralgia. Occasional
(12%–8%): Rash, diarrhea, constipation,
nausea, abdominal pain, dyspepsia, flu-
risperiDONE
like symptoms, peripheral edema. Rare ris-per-i-done
(5%–3%): Bone pain, sinusitis, asthenia, (Perseris, RisperDAL, RisperDAL
dry eye, tinnitus. Consta, RisperiDONE M-Tab)
ADVERSE EFFECTS/TOXIC j BLACK BOX ALERT jIncreased
risk of mortality in elderly pts with
REACTIONS dementia-related psychosis, mainly
Overdose produces hypocalcemia, hypo­ due to pneumonia, HF.
phosphatemia, significant GI distur- Do not confuse RisperDAL with
bances, osteonecrosis of jaw. Restoril, or risperiDONE with
rOPINIRole.
NURSING CONSIDERATIONS uCLASSIFICATION
BASELINE ASSESSMENT PHARMACOTHERAPEUTIC: Benzisox-
Assess symptoms of Paget’s disease (bone azole derivative. CLINICAL: Second-
pain, bone deformities). Hypocalcemia, generation (atypical) antipsychotic.
vitamin D deficiency must be corrected Antimanic agent.
before therapy begins. Obtain baseline
laboratory studies, esp. serum electro- USES
lytes, renal function. Verify pt is able to
stand or sit upright for at least 30 min. Oral: Treatment of schizophrenia, irrita-
R bility/aggression associated with autistic
INTERVENTION/EVALUATION disease in children. Treatment of acute
Check serum electrolytes (esp. calcium, mania associated with bipolar disorder
ionized calcium, phosphorus, alkaline (monotherapy in children and adults; in
phosphatase levels). Monitor I&O, BUN, combination with lithium or valproate in
creatinine in pts with renal impairment. adults). IM: Management of schizophrenia,
maintenance treatment of bipolar 1 disor-
PATIENT/FAMILY TEACHING der (monotherapy or in combination with
• Expected benefits occur only when lithium or valproate in adults). OFF-LABEL:
medication is taken with full glass (6–8 Tourette’s syndrome. Post-traumatic stress
oz) of plain water first thing in the morn- syndrome. Major depressive disorder.
ing and at least 30 min before first food,
beverage, medication of the day. Any PRECAUTIONS
other beverage (mineral water, orange Contraindications: Hypersensitivity to
juice, coffee) significantly reduces ab- risperiDONE. Cautions: Renal/hepatic
sorption of medication. • Do not lie impairment, seizure disorder, cardiac
down for at least 30 min after taking disease, recent MI, breast cancer or
medication (potentiates delivery to stom- other prolactin-dependent tumors,
ach, reduces risk of esophageal irrita- suicidal pts, pts at risk for aspiration
tion). • Report swallowing difficulties, pneumonia. Parkinson’s disease, pts at

underlined – top prescribed drug


risperiDONE 1023
risk for orthostatic hypotension, elderly AVAILABILITY (Rx)
pts, diabetes, decreased GI motility, uri- Injection, Powder for Reconstitution: (Ris­
nary retention, BPH, xerostomia, visual perDAL Consta): 12.5 mg, 25 mg, 37.5 mg,
problems, pts exposed to temperature 50 mg. Oral Solution: 1 mg/mL. Syringe,
extremes, preexisting myelosuppression, Prefilled: 90 mg, 120 mg. Tablets: 0.25
narrow-angle glaucoma; pts with high mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg.
risk of suicide.
Tablets, Orally Disintegrating: 0.25
ACTION mg, 0.5 mg, 1 mg, 2 mg, 3 mg, 4 mg.
May antagonize DOPamine, serotonin ADMINISTRATION/HANDLING
receptors in both CNS and periphery.
b ALERT c Do not administer via IV
Therapeutic Effect: Suppresses psy-
route.
chotic behavior.
IM
PHARMACOKINETICS
Reconstitution • Use only diluent
Well absorbed from GI tract; unaffected and needle supplied in dose pack.
by food. Protein binding: 90%. Metabo- • Prepare suspension according to
lized in liver. Primarily excreted in urine. manufacturer’s directions. • May be
Half-life: 3–20 hrs; metabolite, 21–30 given up to 6 hrs after reconstitution, but
hrs (increased in elderly). Injection: immediate administration is recom-
3–6 days. mended. • If 2 min pass between
reconstitution and injection, shake
LIFESPAN CONSIDERATIONS
upright vial vigorously back and forth to
Pregnancy/Lactation: Unknown if drug resuspend solution.
crosses placenta or is distributed in breast Rate of administration • Inject IM
milk. Breastfeeding not recommended. into upper outer quadrant of gluteus
Children: Safety and efficacy not estab- maximus or into deltoid muscle in upper
lished in children younger than 13 yrs for arm.
schizophrenia, 10 yrs for bipolar mania, and Storage • Store at room temperature.
5 yrs for autistic disorder. Elderly: More
susceptible to postural hypotension. Age- PO
related renal/hepatic impairment may • Give without regard to food. • May R
require dosage adjustment. mix oral solution with water, coffee,
orange juice, low-fat milk. Do not mix
INTERACTIONS with cola, tea.
DRUG: Alcohol, other CNS depres-
sants (e.g., LORazepam, mor- Orally Disintegrating Tablet
phine, zolpidem) may increase CNS • Remove from blister pack immedi-
depression. Strong CYP3A4 inducers ately before administration. • Using
(e.g., carBAMazepine, phenytoin, gloves, place immediately on tongue.
rifAMPin) may decrease concentration/ • Tablet dissolves in seconds. • Pt may
effect. Anticholinergics (e.g., aclidin- swallow with or without liquid. • Do
ium, ipratropium, tiotropium, ume- not split or chew.
clidinium) may increase anticholinergic SQ
effect. HERBAL: Herbals with sedative Insert needle subcutaneously into abdomen
properties (e.g., chamomile, kava only and inject solution. • Do not inject
kava, valerian) may increase CNS into areas of active skin disease or injury
depression. FOOD: None known. LAB such as sunburns, skin rashes, inflamma-
VALUES: May increase serum prolac- tion, skin infections, or active psoria-
tin, glucose, AST, ALT. May cause ECG sis. • Rotate injection sites. • Do not
changes. rub injection site.
Canadian trade name Non-Crushable Drug High Alert drug
1024 risperiDONE

INDICATIONS/ROUTES/DOSAGE SIDE EFFECTS


Schizophrenia Frequent (26%–13%): Agitation, anxi-
PO: ADULTS: Initially, 1–2 mg/day as ety, insomnia, headache, constipation.
single or 2 divided doses. May increase Occasional (10%–4%): Dyspepsia, rhi-
gradually (1–2 mg/day at intervals of at nitis, drowsiness, dizziness, nausea,
least 24 hrs). Usual dosage range: 2–6 mg/ vomiting, rash, abdominal pain, dry
day. ELDERLY: Initially, 0.5 mg twice daily. skin, tachycardia. Rare (3%–2%): Visual
May increase slowly at increments of no disturbances, fever, back pain, pharyngi-
more than 0.5 mg twice daily. Range: 2–6 tis, cough, arthralgia, angina, aggressive
mg/day. CHILDREN 13–17 YRS: Initially, 0.5 behavior, orthostatic hypotension, breast
mg/day (as single daily dose). May increase swelling.
by 0.5–1 mg/day at intervals of greater than
24 hrs to recommended dose of 3 mg/day. ADVERSE EFFECTS/TOXIC
IM: ADULTS, ELDERLY: Initially, 12.5–25 REACTIONS
mg q2wks. Maximum: 50 mg q2wks. Rare reactions include tardive dyskine-
Dosage adjustments should not be made sia (characterized by tongue protrusion,
more frequently than every 4 wks. puffing of the cheeks, chewing or puck-
SQ: ADULTS, ELDERLY: 90–120 mg once ering of mouth), neuroleptic malignant
monthly. syndrome (hyperpyrexia, muscle rigidity,
altered mental status, irregular pulse or
Bipolar Mania
B/P, tachycardia, diaphoresis, cardiac
PO: ADULTS: Initially, 1–3 mg in 1 or 2 arrhythmias, rhabdomyolysis, acute
divided doses. May increase by 1 mg/day renal failure). Hyperglycemia, life-
at 24-hr intervals. Usual dose: 4–6 mg/day. threatening events such as ketoacidosis
ELDERLY: Initially, 0.5 mg twice daily. Titrate
and hyperosmolar coma, death have
slowly. been reported.
PO: CHILDREN 10–17 YRS: Initially, 0.5
mg/day. May increase by 0.5–1 mg/day at NURSING CONSIDERATIONS
intervals of greater than 24 hrs to recom-
mended dose of 2.5 mg/day. IM: ADULTS, BASELINE ASSESSMENT
ELDERLY: 25 mg q2wks. May increase dose Renal function test, LFT should be per-
R in increments of 12.5 mg no sooner than 4 formed before therapy begins. Assess
wks. Maximum: 50 mg q2wks. behavior, appearance, emotional status,
response to environment, speech pattern,
Autism thought content, baseline weight. Obtain
CHILDREN 5 YRS AND OLDER WEIGHING fasting serum glucose, CBC.
MORE THAN 19 KG: Initially, 0.5 mg/day. May
increase to 1 mg after 4 days. May further INTERVENTION/EVALUATION
increase dose by 0.5 mg/day in greater Monitor B/P, heart rate, weight, LFT,
than 2-wk intervals. Range: 0.5–3 mg/day. ECG. Monitor for fine tongue movement
CHILDREN 5 YRS AND OLDER WEIGHING 15–19 (may be first sign of tardive dyskinesia,
KG: Initially, 0.25 mg/day. May increase which may be irreversible). Monitor for
to 0.5 mg/day after 4 days. May further suicidal ideation. Assess for therapeutic
increase dose by 0.25 mg/day in greater response (greater interest in surround-
than 2-wk intervals. Range: 0.5–3 mg/day. ings, improved self-care, increased ability
to concentrate, relaxed facial expression).
Dosage in Renal/Hepatic Impairment
Monitor for potential neuroleptic malig-
Mild to moderate impairment: No
nant syndrome: fever, muscle rigidity, ir-
dose adjustment. Severe impairment: regular B/P or pulse, altered mental status.
Initial dosage for adults, elderly pts is 0.5 Monitor fasting serum glucose periodically
mg twice daily. Dosage is titrated slowly to during therapy.
desired effect.
underlined – top prescribed drug
riTUXimab 1025
PATIENT/FAMILY TEACHING low-grade B-cell NHL; diffuse large B-cell
• Avoid tasks that may require alertness, NHL, previously untreated. Treatment of
motor skills until response to drug is es- CD20-positive chronic lymphocytic leuke-
tablished (may cause dizziness/drowsi- mia (CLL), in combination with fludarabine
ness). • Avoid alcohol. • Go from lying and cyclophosphamide (FC). Treatment
to standing slowly. • Report trembling in of adults with moderate to severe active
fingers, altered gait, unusual muscular/ rheumatoid arthritis (RA), in combina-
skeletal movements, palpitations, severe tion with methotrexate, who have had an
dizziness/fainting, swelling/pain in breasts, inadequate response to one or more TNF
visual changes, rash, difficulty breathing. antagonists. Treatment of granulomatosis
with polyangiitis (GPA) (Wegener’s granu-
lomatosis) and microscopic polyangiitis
(MPA). Treatment of moderate to severe
riTUXimab pemphigus vulgaris. OFF-LABEL: Treatment
of autoimmune hemolytic anemia, chronic
ri-tux-i-mab immune thrombocytopenic purpura (ITP),
(Rituxan, Rituxan Hycela) systemic autoimmune disease (other than
j BLACK BOX ALERT jProfound, rheumatoid arthritis), Burkitt’s lymphoma,
occasionally fatal infusion-related CNS lymphoma, Hodgkin’s lymphoma.
reactions reported during first Rituxan Hycela: Treatment of adults with
30–120 min of first infusion. Tumor relapsed or refractory follicular lymphoma
lysis syndrome leading to acute
renal failure may occur 12–24 as a single agent; previously untreated fol-
hrs following first dose. Severe, licular lymphoma, in combination with
sometimes fatal, mucocutaneous first-line chemotherapy and, in pts achiev-
reactions resulting in progressive ing a complete or partial response to ritux-
multifocal leukoencephalopathy imab in combination with chemotherapy,
(PML) and death reported. Test all
pts for hepatitis B virus (HBV) infec- as a single agent; nonprogressing (includ-
tion prior to initiation. HBV reactiva- ing stable disease) follicular lymphoma as
tion may cause fulminant hepatitis, a single agent after first-line cyclophospha-
hepatic failure, and death. mide, vincristine and predniSONE chemo-
Do not confuse Rituxan with therapy. Treatment of adults with diffuse
Remicade, or riTUXimab with large B-cell lymphoma in adults (previous R
bevacizumab, inFLIXimab, untreated) in combination with cyclo-
brentuximab, obinutuzumab, phosphamide, doxorubicin, vincristine,
ofatumumab, ramucirumab, predniSONE, or other anthracycline-based
ruxolitinib. chemotherapy regimens. Treatment of
CLL, in combination with fludarabine and
uCLASSIFICATION
cyclophosphamide (previously untreated
PHARMACOTHERAPEUTIC: Anti-CD20 and previously treated CLL). Limitations:
monoclonal antibody. CLINICAL: Dis- Only indicated in pts who have had at least
ease-modifying antirheumatic drug one full dose of intravenous rituximab. Not
(DMARD), antineoplastic, immuno- indicated for treatment of nonmalignant
suppressant. conditions.
PRECAUTIONS
USES
Contraindications: Hypersensitivity to ri-­
RiTUXimab: Treatment of CD20-pos- TUXimab. Cautions: Baseline anemia,
itive non-Hodgkin’s lymphomas (NHL): neutropenia, thrombocytopenia; active
relapsed or refractory, low-grade, or fol- infection, conditions predisposing to
licular B-cell NHL; follicular B-cell NHL infection (e.g., diabetes, renal fail-
(previously untreated); nonprogressive, ure, immunocompromised pts, open

Canadian trade name Non-Crushable Drug High Alert drug


1026 riTUXimab
wounds); pts at risk for tumor lysis syn- immunosuppressive effect. May increase
drome (high tumor burden). History of immunosuppressive effect of fingoli-
cardiac disease, elderly pts, pulmonary mod. May decrease concentration/effect
disease, renal impairment, hepatitis B of nivolumab, sipuleucel-T. Trastu-
virus (HBV) infection, hepatitis C virus zumab may increase neutropenic effect.
(HCV) infection; pts at risk for GI perfo- May decrease therapeutic effect; increase
ration (Crohn’s disease, diverticulitis, GI risk of adverse effect of live vaccines.
tract malignancies, peptic ulcers, perito- HERBAL: Echinacea may decrease
neal malignancies). Avoid administration therapeutic effect. FOOD: None known.
of live or live attenuated vaccines during LAB VALUES: May increase serum cre-
treatment and after discontinuation until atinine, glucose; LDH. May decrease Hgb,
B cells are no longer depleted. Hct, leukocytes, lymphocytes, neutrophils,
platelets, RBCs; B-cell counts, immuno-
ACTION globulin concentrations. May diminish
Binds to CD20, the antigen found on sur- diagnostic effect of Coccidioides immitis
face of B lymphocytes. Activates B-cell skin test.
cytotoxicity. B cells may also play a role
in development/progression of RA. Hyal- AVAILABILITY (Rx)
uronidase increases the absorption rate Injection Solution, IV: 10 mg/mL (10 mL,
of rituximab by increasing permeability 50 mL). Injection Solution, SQ: (Rituxan
of SQ tissue.  Therapeutic Effect: Pro- Hycela): 1,400 mg/23,400 units, 1,600
duces cytotoxicity, reduces tumor size. mg/26,800 units.
Signs/symptoms of rheumatoid arthritis
are reduced; structural damage delayed. ADMINISTRATION/HANDLING
IV
PHARMACOKINETICS
Rapidly depletes B cells. Half-life: 59.8 b ALERT c Do not give by IV push or
hrs after first infusion, 174 hrs after bolus. Must be administered by a health
fourth infusion. care professional who is experienced
in management of severe infusion reac-
LIFESPAN CONSIDERATIONS tions.
R Pregnancy/Lactation: May cause fetal Reconstitution • Dilute with 0.9%
harm due to fetal B-cell depletion and NaCl or D5W to provide final concentra-
lymphocytopenia in neonates. Unknown tion of 1–4 mg/mL in infusion bag.
if distributed in breast milk. Females of Rate of administration • Initially infuse
reproductive potential should use effective at rate of 50 mg/hr. If no hypersensitivity or
contraception during treatment and for up infusion-related reaction, may increase infu-
to 12 mos after discontinuation. Breastfeed- sion rate in 50 mg/hr increments q30min to
ing not recommended during treatment maximum 400 mg/hr. • Subsequent infu-
and for at least 6 mos after discontinua- sion can be given at 100 mg/hr and
tion. Children: Safety and efficacy not increased by 100 mg/hr increments q30min
established. Elderly: Increased risk of to maximum 400 mg/hr.
cardiac/pulmonary adverse reactions. Storage • Refrigerate vials. • Diluted
solution is stable for 24 hrs if refrigerated
INTERACTIONS or at room temperature.
DRUG: Denosumab, pimecroli-
SQ
mus, tacrolimus may increase risk
of adverse effects. May increase toxic Preparation • Visually inspect for
effects of abatacept, belimumab, particulate matter or discoloration. Solu-
clozapine, leflunomide, natali- tion should appear clear to opalescent,
zumab. Roflumilast may increase colorless to slightly yellow in color. Do

underlined – top prescribed drug


riTUXimab 1027
not use if solution is cloudy, discolored, NHL (Follicular, CD20-Positive, B-cell,
or if visible particles are observed. Previously Untreated)
Administration • For 1,400 mg/ IV: ADULTS: 375 mg/m2 on day 1 of
23,400 unit dose (11.7 mL), insert nee- each cycle up to 8 doses. Maintenance
dle subcutaneously into abdomen and (single agent): 375 mg/m2 q8wks for
inject solution over 5 min. • For 1,600 12 doses.
mg/26,800 unit dose (13.4 mL), insert SQ: ADULTS: 1,400 mg/23,400 units
needle subcutaneously into abdomen on day 1 of cycles 2–8 (q21 days), for
and inject solution over 7 min. • Do up to 7 cycles following full dose of IV
not inject into areas of active skin disease rituximab on day 1 of cycle 1 (e.g., up
or injury such as sunburns, skin rashes, to 8 cycles total). In pts with partial or
inflammation, skin infections, or active complete response, start maintenance
psoriasis. • If administration is inter- therapy 8 wks after completion. Admin-
rupted, continue administering at the ister as single agent q8wks for 12 doses.
same site (or at different site) but only in
the SQ abdomen. • Do not administer NHL (Nonprogressive, CD20-Positive,
IV or intramuscular. • Rotate injection B-cell Following 6–8 Cycles of
sites. Cyclophosphamide, VinCRIStine, and
Storage • Refrigerate unused vials PrednisoLONE [CVP Therapy])
until time of use. • Protect from light. IV: ADULTS: 375 mg/m2 once wkly for
• Do not freeze or expose to heating 4 doses q6mos. Maximum: 16 doses.
sources. • Once transferred to syringe, SQ: ADULTS: 1,400 mg/23,400 units
may refrigerate for up to 48 hrs or store at once wkly for 3 wks (e.g., 4 wks total)
room temperature for up to 8 hrs. at 6-mo intervals following completion of
CVP therapy and a full dose of IV ritux-
IV INCOMPATIBILITIES imab at wk 1. Maximum: 16 doses.
Do not mix with any other medications. NHL (Combination with Ibritumomab)
IV: ADULTS: 250 mg/m2 day 1; repeat in
INDICATIONS/ROUTES/DOSAGE
NHL (Relapsed/Refractory, Low-Grade or
7–9 days with ibritumomab.
Follicular CD20-Positive B-cell) Rheumatoid Arthritis
IV: ADULTS: 375 mg/m2 wkly for 4 or 8 IV: ADULTS: 1,000 mg every 2 wks times R
doses. 2 doses in combination with metho-
SQ: ADULTS: 1,400 mg/23,400 units trexate. May repeat course q24wks (if
once wkly for 3 or 7 wks following full needed, no sooner than 16 wks).
dose of IV rituximab at wk 1 (e.g., 4 or 8
wks total). ADULTS (RETREATMENT): 1,400 CLL
mg/23,400 units once wkly for 3 wks fol- IV: ADULTS: 375 mg/m2 in first cycle
lowing full dose of IV rituximab at wk 1 (on day prior to fludarabine/cyclophos-
(e.g., 4 wks total). phamide) and 500 mg/m2 on day 1 in
cycles 2–6, administered every 28 days.
NHL (Diffuse Large B-cell) SQ: ADULTS: 1,600 mg/26,800 units on
IV: ADULTS: 375 mg/m2 on day 1 of day 1 of cycles 2–6 (q28 days) for a total
each cycle up to 8 doses. of 5 cycles following full dose of IV ritux-
SQ: ADULTS: 1,400 mg/23,400 units imab on day 1 of cycle 1 (e.g., 6 cycles
on day 1 of cycles 2–8 of CHOP chemo- total).
therapy for up to 7 cycles following full
dose of IV rituximab at day 1, cycle 1 of GPA, MPA
CHOP therapy. 375 mg/m2 once wkly
IV: ADULTS:
for 4 wks (in combination with

Canadian trade name Non-Crushable Drug High Alert drug


1028 riTUXimab
methylPREDNISolone IV for 1–3 days, nasopharyngitis, bronchitis, UTI, sinus-
then daily predniSONE). itis, conjunctivitis, influenza occurred in
15%–4% of pts. May cause HBV reacti-
Pemphigus vulgaris vation, resulting in fulminant hepatitis,
IV: ADULTS, ELDERLY: 1,000 mg q2wks for hepatic failure, and death. Tumor lysis
2 doses (in combination with a tapering syndrome may present as acute renal
course of glucocorticoids), then 500 mg at failure, hypocalcemia, hyperuricemia,
months 12 and 18 and q6mos thereafter. hyperphosphatemia. Fatal cases of bowel
perforation/obstruction were reported.
Dosage in Renal/Hepatic Impairment
No dose adjustment. NURSING CONSIDERATIONS
SIDE EFFECTS BASELINE ASSESSMENT
Note: Side effects may vary depending Obtain CBC; pregnancy test in females of
on dose and indicated treatment. Fre- reproductive potential; LFT in pts with
quent (53%–14%): Fever, chills, asthenia, history of HCV, HBV infection. Test all
constipation, nausea, headache, pares- pts for hepatitis B virus infection. Initiate
thesia, night sweats, pyrexia, rash, pruri- anti-HBV therapy if warranted. Recom-
tus, abdominal pain, alopecia. Occasional mend continuous ECG monitoring during
(13%–5%): Cough, pain, rhinitis, periph- initial infusions. Screen for active infec-
eral neuropathy, back pain, bone pain, tion. Pretreatment with acetaminophen
diarrhea, vomiting, dizziness, myalgia, and diphenhydrAMINE before each infu-
arthralgia, hypotension, insomnia, ery- sion may prevent infusion-related effects.
thema, throat irritation, urticaria, muscle Confirm compliance of effective contra-
spasm, dyspnea, hypertension, chest pain, ception. Conduct baseline dermatologi-
flushing, anxiety, peripheral edema. cal exam and assess skin for open/un-
healed wounds, lesions, moles. Receive
ADVERSE EFFECTS/ full medication history and screen for
TOXIC REACTIONS interactions. Question history of cardiac
Anemia, leukopenia, lymphopenia, neu- disease, GI perforation, chronic infec-
tropenia, thrombocytopenia are expected tions, renal impairment. All pts planning
R responses to therapy. Severe infusion to receive SQ dose must complete at least
reactions including anaphylaxis, angio- one full intravenous dose. Recommend
edema, ARDS, bronchospasm, hypo- prophylactic treatment for Pneumocystis
tension, hypoxia, pulmonary infiltrates jiroveci (PCP) and herpes virus infection
were reported. Cardiac events including in pts with CLL during treatment and for
cardiogenic shock, MI, ventricular fibril- up to 12 mos after discontinuation. Offer
lation may occur, particularly in pts with emotional support.
history of preexisting cardiac conditions. INTERVENTION/EVALUATION
Severe, and sometimes fatal, mucocuta-
neous reactions including paraneoplastic Monitor CBC at regular intervals. Monitor
pemphigus, Stevens-Johnson syndrome, serum calcium, phosphate, uric acid if
lichenoid dermatitis, vesiculobullous tumor lysis syndrome is suspected (acute
dermatitis, toxic epidermal necrolysis renal failure, electrolyte imbalance, car-
may occur. Progressive multifocal leu- diac arrhythmias, seizures). Monitor
koencephalopathy (PML), an opportu- for infections of any kind. Monitor for
nistic viral infection of the brain caused an infusion-related reaction; generally
by the JC virus, may result in progres- occurs within 30 min–2 hrs of beginning
sive permanent disability and death. first infusion. Slowing infusion resolves
Infections including upper respiratory symptoms. If given SQ, monitor pt at
tract infection, pneumonia, pharyngitis, least 15 min following administration. Pts
who present with abdominal pain, fever,
underlined – top prescribed drug
rivaroxaban 1029
nausea, vomiting should be evaluated for HBV reactivation (fatigue, yellowing of
bowel perforation/obstruction. Assess the skin or eyes); bowel obstruction or
mouth for ulcerations; skin for cutane- perforation (abdominal pain, fever, nau-
ous reactions. Closely monitor for exac- sea, vomiting); cardiovascular events
erbation of hepatitis or HBV reactivation (chest pain, cold/clammy skin, difficulty
(amber- to orange-colored urine, fatigue, breathing, fainting, irregular heartbeat,
jaundice, nausea, vomiting). Due to risk palpitations, sweating). • Do not take
of cardiovascular events, have emergency newly prescribed medications unless ap-
resuscitation equipment ready available. proved by the prescriber who originally
Offer antiemetic if nausea occurs, antidi- started treatment.
arrheal if diarrhea occurs. Monitor daily
pattern of bowel activity, stool consis-
tency. Ensure adequate hydration, nutri-
tion. Monitor weight, I&Os rivaroxaban
PATIENT/FAMILY TEACHING
rye-va-rox-a-ban
• Treatment may depress the immune (Xarelto)
system and reduce the ability to fight in- j BLACK BOX ALERT jEpidural/
fection. Report symptoms of infection spinal hematomas may occur in pts
such as body aches, burning with urina- receiving neuraxial anesthesia or
tion, chills, cough, fatigue, fever. Avoid spinal puncture, resulting in long-
those with active infection. • Therapy term or permanent paralysis. Factors
increasing risk of epidural/spinal he-
may cause tumor lysis syndrome (a con- matoma include indwelling epidural
dition caused by the rapid breakdown of catheters, concomitant drugs such
cancer cells), which can cause kidney as NSAIDs, platelet inhibitors, other
failure and can be fatal. Report de- anticoagulants; history of traumatic
creased urination, amber-colored urine, or repeated spinal or epidural punc-
tures, history of spinal deformity or
confusion, difficulty breathing, fatigue, spinal surgery. Monitor for signs and
fever, muscle or joint pain, palpitations, symptoms of neurologic impairment.
seizures, vomiting. • Report symptoms Consider benefits and risks before
of bone marrow depression such as neuraxial intervention in anticoagu-
bruising, fatigue, fever, shortness of lated pts or planned thromboprophy-
laxis. Increased risk of stroke may R
breath, weight loss; bleeding easily, occur in pts with atrial fibrillation
bloody urine or stool. • Treatment may when discontinuing for reasons
cause fetal harm. Use effective contracep- other than bleeding.
tion during treatment and for at least 12 Do not confuse rivaroxaban
mos after last dose. Breastfeeding not with argatroban.
recommended during treatment and for
at least 6 mos after last dose. • PML, an uCLASSIFICATION
opportunistic viral infection of the brain, PHARMACOTHERAPEUTIC: Factor Xa
may cause progressive, permanent dis- inhibitor. Direct oral anticoagulant.
abilities and death. Report symptoms of CLINICAL: Anticoagulant.
PML, brain hemorrhage such as confu-
sion, memory loss, paralysis, trouble
speaking, vision loss, seizures, weak- USES
ness. • Immediately report symptoms Prophylaxis of deep vein thrombosis (DVT)
of infusion reactions (difficulty breath- in pts undergoing knee or hip replacement
ing, itching, hives, palpitations, rash, surgery. Prevents stroke/systemic embo-
swelling of the face or tongue); severe lism in pts with nonvalvular atrial fibrilla-
mucocutaneous reactions (blisters, peel- tion. Treatment of DVT/PE. Reduces risk
ing of skin, ulceration of the mouth); of recurrent DVT/PE following 6 mos of

Canadian trade name Non-Crushable Drug High Alert drug


1030 rivaroxaban
treatment. In combination with aspirin, clopidogrel), NSAIDs (e.g., ibupro-
reduces risk of major CV events (e.g., MI, fen, ketorolac, naproxen) may increase
stroke) in pts with chronic coronary artery bleeding risk. Apixaban, dabigatran,
disease (CAD) or peripheral artery disease edoxaban may increase anticoagulant
(PAD). effect. HERBAL: Herbals with anticoagu-
lant/antiplatelet properties (e.g., gar-
PRECAUTIONS lic, ginger, ginkgo biloba) may increase
Contraindications: Hypersensitivity to risk of bleeding. FOOD: Grapefruit prod-
rivaroxaban. Active major bleeding. Cau- ucts may increase risk of bleeding. LAB
tions: Renal/hepatic impairment, pts at VALUES: May decrease platelets. May
increased risk of bleeding (e.g., throm- increase serum ALT, AST, bilirubin.
bocytopenia, stroke, severe uncontrolled
hypertension), elderly pts; avoid use with AVAILABILITY (Rx)
heparin, low molecular weight heparin Tablets: 10 mg, 15 mg, 20 mg.
(LMWH), aspirin, warfarin, NSAIDs. Pts
with prosthetic heart valves or significant ADMINISTRATION/HANDLING
rheumatic heart disease. PO
• Administer doses of 15 mg or greater
ACTION with food; doses of 10 mg/day may be
Selectively and reversibly blocks active given without regard to food. • DVT
site of factor Xa, a key factor in the intrin- prophylaxis (knee, hip): Give without
sic and extrinsic pathway of blood coagu- regard to food. • Nonvalvular atrial
lation cascade. Inhibits platelet activation fibrillation: Give with evening meal.
and fibrin clot formation. Therapeutic
Effect: Inhibits blood coagulation. INDICATIONS/ROUTES/DOSAGE
Note: Avoid in pts with BMI greater than
PHARMACOKINETICS 40 kg/m2 or weight greater than 120 kg due
Rapidly absorbed after PO administra- to lack of clinical data in this population.
tion. Peak plasma concentration: 2–4 hrs.
Absorption dependent on site of drug release DVT Prophylaxis, Knee Replacement
within GI tract. Avoid administration into PO: ADULTS: 10 mg daily for minimum
R small intestine due to reduced absorption. 10–14 days up to 35 days. Initiate at least
Protein binding: 92%–95%. Metabolized in 6–10 hrs after surgery once hemostasis
liver. Excreted in urine (66%), feces (28%). established. CrCl less than 30 mL/
Half-life: 5–9 hrs, 11–13 hrs (elderly pts). min: Avoid use.

LIFESPAN CONSIDERATIONS DVT Prophylaxis, Hip Replacement


PO: ADULTS: 10 mg daily for 10–14
Pregnancy/Lactation: Crosses placenta.
Use during pregnancy should be avoided. days (minimum) up to 35 days. Initi-
Unknown if excreted in breast milk. Chil- ate at least 6–10 hrs after surgery once
dren: Safety and efficacy not established.
hemostasis established. CrCl less than
Elderly: May be at increased risk for
30 mL/min: Avoid use.
bleeding due to age-related renal impair- Nonvalvular Atrial Fibrillation
ment. Use caution. PO: ADULTS: CrCl greater than 50
INTERACTIONS mL/min: 20 mg daily. CrCl 15–50 mL/
min: 15 mg daily. CrCl less than 15
DRUG: Strong CYP3A4 inhibitors (e.g., mL/min: Avoid use.
ketoconazole, clarithromycin, ritona-
vir) may increase concentration, risk of Treatment of DVT/PE
bleeding. Anticoagulants (e.g., heparin, PO: ADULTS, ELDERLY: 15 mg twice daily
warfarin), antiplatelets (e.g., aspirin, for 3 wks, then 20 mg once daily.
underlined – top prescribed drug
rivastigmine 1031
Reduce Risk of DVT/PE (After 6 mos INTERVENTION/EVALUATION
Treatment) Monitor CBC, serum chemistries, renal
PO: ADULTS, ELDERLY: 10 mg once daily function, occult urine/stool. Be alert for
up to 6–12 mos. complaints of abdominal/back pain, head-
ache, confusion, weakness, vision change
Reduce Risk of CV Events
(may indicate hemorrhage). Question for
PO: ADULTS, ELDERLY: 2.5mg twice daily increased menstrual bleeding/discharge.
(in combination with aspirin [75–100 Assess peripheral pulses; skin for ec-
mg] once daily). chymosis, petechiae. Check for excessive
Dosage in Renal Impairment bleeding from minor cuts, scratches. As-
CrCl less than 30 mL/min: Avoid use sess urine output for hematuria. Immedi-
in DVT/PE, postoperative thrombopro- ately report suspected pregnancy.
phylaxis. Nonvalvular atrial fibril- PATIENT/FAMILY TEACHING
lation: CrCl 15–50 mL/min: 15 mg
• Do not take/discontinue any medication
once daily with evening meal. CrCl less except on advice of physician. • Avoid
than 15 mL/min: Avoid use.
alcohol, aspirin, NSAIDs. • Consult phy-
Dosage in Hepatic Impairment sician before surgery, dental work. • Use
Mild impairment: No dose adjustment. electric razor, soft toothbrush to prevent
Moderate to severe impairment: bleeding. • Report any unusual bleed-
Avoid use. ing/bruising, spinal/epidural hematomas
(e.g., tingling, numbness, muscular weak-
SIDE EFFECTS ness). • Report if pregnant or planning
Rare (3%–1%): Wound secretion/oozing, to become pregnant. • Avoid grapefruit
extremity pain, muscle spasm, syncope, products.
pruritus.
ADVERSE EFFECTS/TOXIC
REACTIONS
rivastigmine
Increased risk of bleeding/hemorrhagic riv-a-stig-meen
events including retroperitoneal hemor- (Exelon)
rhage, cerebral hemorrhage, subdural R
hematoma, epidural/spinal hematoma uCLASSIFICATION
(esp. with epidural catheters, spinal PHARMACOTHERAPEUTIC: Acetylcho-
trauma). Serious reactions including linesterase inhibitor. CLINICAL: Anti-
jaundice, cholestasis, cytolytic hepatitis, Alzheimer’s dementia agent.
Stevens-Johnson syndrome, hypersensi-
tivity reaction, anaphylaxis reported.
USES
NURSING CONSIDERATIONS Oral: Treatment of mild to moder-
BASELINE ASSESSMENT ate dementia of Alzheimer’s or mild to
moderate dementia of Parkinson’s disease.
Obtain CBC, serum chemistries, PT/INR,
Transdermal: Treatment of mild, moder-
vital signs, urine pregnancy if applicable.
ate, or severe dementia of the Alzheimer
Obtain ECG for pts with a history of atrial
type. Treatment of mild to moderate demen-
fibrillation. Question for history of bleed-
tia associated with Parkinson’s disease.
ing disorders, recent surgery, spinal punc-
OFF-LABEL: Lewy body dementia.
tures, intracranial hemorrhage, bleeding
ulcers, open wounds, anemia, renal/he- PRECAUTIONS
patic impairment. Receive full medication
Contraindications: Hypersensitivity to
history including herbal products.
riv­astigmine, other carbamate derivatives
Canadian trade name Non-Crushable Drug High Alert drug
1032 rivastigmine
(e.g., neostigmine), history of applica- Transdermal Patch
tion site reactions with rivastigmine • May apply the day following the last
patch. Cautions: Peptic ulcer disease, oral dose. • Apply to upper or lower
concurrent use of NSAIDs, sick sinus syn- back, upper arm, or chest. • Avoid reap-
drome, bradycardia or supraventricular plication to same spot of skin for 14
conduction defects, urinary obstruction, days. • Do not apply to red, irritated,
seizure disorders, asthma, COPD, pts or broken skin. • Avoid eye contact.
with body weight less than 50 kg. • After removal, fold patch to press adhe-
sive together and discard.
ACTION
Increases acetylcholine in CNS by revers- INDICATIONS/ROUTES/DOSAGE
ibly inhibiting hydrolysis by cholines- Alzheimer’s Dementia (Mild to Moderate)
terase. Therapeutic Effect: Slows PO: ADULTS, ELDERLY: Initially, 1.5 mg
progression of symptoms of Alzheimer’s twice daily. May increase at intervals of at
disease, dementia of Parkinson’s disease. least 2 wks to 3 mg twice daily, then 4.5
mg twice daily, and finally 6 mg twice daily.
PHARMACOKINETICS Maximum: 6 mg twice daily.
Rapidly, completely absorbed. Pro- Transdermal: Initially, 4.6 mg/24 hrs.
tein binding: 40%. Widely distributed May increase at intervals of at least 4 wks to
throughout body. Rapidly, extensively 9.5 mg/24 hrs and then to 13.3 mg/24 hrs.
metabolized. Primarily excreted in urine.
Half-life: 1.5 hrs. Alzheimer’s Dementia (Severe)
Transdermal: ADULTS, ELDERLY: Ini-
LIFESPAN CONSIDERATIONS tially, 4.6 mg/24 hrs. May increase at
Pregnancy/Lactation: Unknown if intervals of at least 4 wks to 9.5 mg/24
distributed in breast milk. Children: Not hrs and then to 13.3 mg/24 hrs.
indicated for use in this pt population. Parkinson’s Dementia
Elderly: No age-related precautions
PO: ADULTS, ELDERLY: Initially, 1.5 mg
noted. twice daily. May increase at intervals of
INTERACTIONS at least 4 wks to 3 mg twice daily, then
4.5 mg twice daily, and finally 6 mg twice
R DRUG: May interfere with anticholiner- daily. Maximum: 6 mg twice daily.
gics (e.g., dicyclomine, glycopyrro- Transdermal: Initially, 4.6 mg/24 hrs.
late, scopolamine) effects. May increase May increase after 4 wks to 9.5 mg/24 hrs
the bradycardic effect of beta blockers and then to 13.3 mg/24 hrs.
(e.g., atenolol, carvedilol, metopro-
lol). May increase the adverse effects of Dosage in Renal Impairment
metoclopramide. HERBAL: None sig- No dose adjustment.
nificant. FOOD: None known. LAB VAL-
UES: None significant. Dosage in Hepatic Impairment
Oral: No dose adjustment.
AVAILABILITY (Rx) Transdermal: Maximum: 4.6 mg/24 hrs.
Transdermal Patch: 4.6 mg/24 hrs, 9.5
mg/24 hrs, 13.3 mg/24 hrs. SIDE EFFECTS
Capsules: 1.5 mg, 3 mg, 4.5 mg, 6 mg. Frequent (47%–17%): Nausea, vomiting,
dizziness, diarrhea, headache, anorexia.
ADMINISTRATION/HANDLING Occasional (13%–6%): Abdominal pain,
PO insomnia, dyspepsia (heartburn, indiges-
• Give morning and evening doses with tion, epigastric pain), confusion, UTI,
food. • Give capsule whole; do not break, depression. Rare (5%–3%): Anxiety, drows-
cut, or open. iness, constipation, malaise, hallucinations,

underlined – top prescribed drug


rizatriptan 1033
tremor, flatulence, rhinitis, hypertension, PRECAUTIONS
flu-like symptoms, weight loss, syncope. Contraindications: Hypersensitivity
to rizatriptan. Basilar or hemiplegic
ADVERSE EFFECTS/TOXIC
migraine, history of stroke or transient
REACTIONS
ischemic attack; severe cardiovascular
Overdose can produce cholinergic crisis, disease, coronary artery vasospasm,
characterized by severe nausea/vomiting, peripheral vascular disease, ischemic
increased salivation, diaphoresis, brady- bowel disease, uncontrolled hyperten-
cardia, hypotension, respiratory depres- sion, use within 24 hrs of ergotamine-
sion, seizures. containing preparations or another
serotonin receptor agonist, MAOI use
NURSING CONSIDERATIONS within 14 days. Cautions: Mild to mod-
BASELINE ASSESSMENT erate renal/hepatic impairment, dialysis
Obtain baseline vital signs. Assess his- pts, elderly pts, pt profile suggesting
tory for peptic ulcer, urinary obstruction, cardiovascular risks (e.g., hypertension,
asthma, COPD, cardiac disease. Assess diabetes, hypercholesterolemia).
cognitive, behavioral, functional deficits. ACTION
INTERVENTION/EVALUATION Binds selectively to serotonin 5-HT1 recep-
Monitor for cholinergic reaction: GI tors in cranial arteries producing vasocon-
discomfort/cramping, feeling of facial striction. Therapeutic Effect: Relieves
warmth, excessive salivation, diaphore- migraine headache.
sis, lacrimation, pallor, urinary urgency,
dizziness. Monitor for nausea, diarrhea, PHARMACOKINETICS
headache, insomnia. Well absorbed after PO administration.
Protein binding: 14%. Crosses blood-
PATIENT/ FAMILY TEACHING brain barrier. Metabolized by liver.
• Take with meals (at breakfast, din- Excreted primarily in urine (82%), feces
ner). • Swallow capsule whole. Do not (12%). Half-life: 2–3 hrs.
break, chew, or divide capsules. • Re-
port nausea, vomiting, diarrhea, diaphore- LIFESPAN CONSIDERATIONS
sis, increased salivary secretions, severe Pregnancy/Lactation: Unknown R
abdominal pain, dizziness. if drug is distributed in breast milk.
Children: Safety and efficacy not
established. Elderly: No age-related
precautions noted.
rizatriptan
INTERACTIONS
rye-za-trip-tan DRUG: Ergot derivatives (e.g., ergot-
(Maxalt, Maxalt-MLT, Maxalt RPD ) amine) may increase vasoconstrictive
effect. Strong CYP3A4 inhibitors
uCLASSIFICATION (e.g., clarithromycin, ketoconazole
PHARMACOTHERAPEUTIC: Serotonin may increase concentration/effect.
5-HT1 receptor agonist. CLINICAL: An- MAOIs (e.g., phenelzine, selegi-
timigraine. line), propranolol may dramatically
increase concentration (avoid concur-
rent use). HERBAL: None significant.
USES FOOD: All foods delay peak drug con-
Treatment of acute migraine headache centration by 1 hr. LAB VALUES: None
with or without aura. significant.

Canadian trade name Non-Crushable Drug High Alert drug


1034 roflumilast

AVAILABILITY (Rx) NURSING CONSIDERATIONS


Tablets (Maxalt): 5 mg, 10 mg. Tablets,
Orally Disintegrating: (Maxalt-MLT): 5 BASELINE ASSESSMENT
mg, 10 mg. Question for history of peripheral vascu-
lar disease, renal/hepatic impairment.
ADMINISTRATION/HANDLING Question pt regarding onset, location,
PO duration of migraine, possible precipitat-
• Orally disintegrating tablet is packaged ing symptoms.
in individual aluminum pouch. • Open INTERVENTION/EVALUATION
packet with dry hands. • Place tablet
onto tongue, allow to dissolve, swallow Monitor for evidence of dizziness. Assess
with saliva. Administration with water is for photophobia, phonophobia (sound
not necessary. sensitivity, nausea, vomiting), relief of
migraine headache.
INDICATIONS/ROUTES/DOSAGE PATIENT/FAMILY TEACHING
Acute Migraine Headache
• Take single dose as soon as symptoms
PO: ADULTS OLDER THAN 18 YRS, ELDERLY:
of an actual migraine headache ap-
5–10 mg. If significant improve­ment is pear. • Medication is intended to relieve
not attained, dose may be repeated after migraine, not to prevent or reduce num-
2 hrs. Maximum: 30 mg/24 hrs. (Use ber of attacks. • Avoid tasks that require
5 mg/dose in pts taking propranolol with alertness, motor skills until response to
maximum of 15 mg/24 hrs.) CHILDREN drug is established. • Report immedi-
6–17 YRS WEIGHING 40 KG OR GREATER: 10
ately if palpitations, pain/tightness in
mg as single dose. (Maximum 5 mg as chest/throat, pain/weakness of extremities
single dose with propranolol.) WEIGH- occurs. • Do not remove orally disinte-
ING LESS THAN 40 KG: 5 mg as a single
grating tablet from blister pack until just
dose. (Not recommended if taking before dosing. • Use protective mea-
propranolol.) sures against exposure to UV light, sun-
Dosage in Renal/Hepatic Impairment light (sunscreen, protective clothing).
No dose adjustment.
R
SIDE EFFECTS roflumilast
Frequent (9%–7%): Dizziness, drowsiness, roe-floo-mi-last
paresthesia, fatigue. Occasional (6%– (Daliresp, Daxas )
3%): Nausea, chest pressure, dry mouth.
Rare (2%): Headache; neck, throat, jaw uCLASSIFICATION
pressure; photosensitivity. PHARMACOTHERAPEUTIC: Phos-
phodiesterase 4 (PDE4) inhibitor.
ADVERSE EFFECTS/TOXIC
CLINICAL: Anti-COPD agent.
REACTIONS
Cardiac reactions (ischemia, coronary
artery vasospasm, MI), noncardiac vaso- USES
spasm-related reactions (hemorrhage, Adjunct to bronchodilator therapy for
CVA) occur rarely, particularly in pts with maintenance treatment of severe COPD
hypertension, diabetes, strong family his- associated with chronic bronchitis and
tory of coronary artery disease, obesity, history of exacerbations.
smokers, males older than 40 yrs, post-
menopausal women. PRECAUTIONS
Contraindications:Hypersensitivity to
roflu­
milast. Moderate to severe hepatic
underlined – top prescribed drug
roflumilast 1035
impairment. Cautions: Mild hepatic daily. Note: 250 mcg dose is not consid-
im­pairment, history of depression, suicidal ered therapeutic (given in attempt to
ideation. Not indicated as ­bronchodilator improve tolerability).
or for relief of acute bronchospasm.
Dosage in Renal Impairment
ACTION No dose adjustment.
Selectively inhibits PDE4, causing an accu- Dosage in Hepatic Impairment
mulation of cyclic AMP within inflammatory/ Mild impairment: No dose adjust-
structural cells necessary in pathogenesis of ment. Moderate to severe impairment:
COPD. Produces anti-inflammatory effects Contraindicated.
(reduces cytokine release, inhibits neu-
SIDE EFFECTS
trophil infiltration in lungs). Therapeutic
Effect: Reduces risk of exacerbation of Occasional (10%–4%): Diarrhea, nausea,
COPD/chronic bronchitis. headache. Rare (3%–2%): Back pain, flu-like
symptoms, insomnia, dizziness, decreased
PHARMACOKINETICS appetite, vomiting, abdominal pain, rhinitis,
Readily absorbed after PO administration. muscle spasm, tremor, dyspepsia.
Maximum plasma concentration: 0.5–2 ADVERSE EFFECTS/TOXIC
hrs. Protein binding: 99%. Metabolized in REACTIONS
liver. Primarily excreted in urine (70%).
Half-life: 17 hrs. Psychiatric events including worsening
depression, suicidal ideation, anxiety
LIFESPAN CONSIDERATIONS reported in less than 2% of pts. Moder-
ate to severe weight loss may result in
Pregnancy/Lactation: Unknown if dis­
discontinuation.
tributed in breast milk. Not recommended
for nursing mothers. Children: Safety NURSING CONSIDERATIONS
and efficacy not established. Elderly: No
­age-related precautions noted. BASELINE ASSESSMENT
Assess vital signs, O2 saturation, lung
INTERACTIONS sounds, body weight. Question for history
DRUG: Strong CYP3A4 inducers (e.g., of depression, anxiety, suicidal ideation,
dehydration, COPD, hepatic impairment. R
carBAMazepine, phenytoin, rifAMPin)
may decrease efficacy. Strong CYP3A4 Assess plans for breastfeeding. Obtain full
inhibitors (e.g., clarithromycin, keto- medication history.
conazole) may increase concentration. INTERVENTION/EVALUATION
HERBAL: St. John’s wort may decrease
concentration/effect. FOOD: None known. Monitor vital signs, O2 saturation, mental
LAB VALUES: None significant. status, body weight. Assess for dehydra-
tion if diarrhea occurs (skin turgor, mu-
AVAILABILITY (Rx) cous membranes, decreased urine output,
Tablets: 250 mcg, 500 mcg. dizziness, dry mouth).
PATIENT/FAMILY TEACHING
ADMINISTRATION/HANDLING • Report changes in mood or behavior,
PO thoughts of suicide, insomnia, anxiety. •
• Give without regard to food. Report any weight loss. • Increase fluid
intake if dehydration is sus-
INDICATIONS/ROUTES/DOSAGE pected. • Worsening cough, fever, diffi-
Adjunct in Severe COPD culty breathing may indicate exacerbation/
PO: ADULTS, ELDERLY: Initially,250 mg infection. • Immediately report if preg-
once daily for 4 wks, then 500 mcg once nancy is suspected.

Canadian trade name Non-Crushable Drug High Alert drug


1036 rolapitant
Children: Safety and efficacy not estab-
rolapitant lished. Elderly: No age-related precau-
tions noted.
roe-la-pi-tant
(Varubi) INTERACTIONS
Do not confuse rolapitant with DRUG: Thioridazine may increase risk
aprepitant, fosaprepitant. of torsades de pointes, QT internal prolon-
uCLASSIFICATION gation (contraindicated). Strong CYP3A
inducers (e.g., carBAMazepine, phe-
PHARMACOTHERAPEUTIC: Substance nytoin, rifAMPin) may decrease concen-
P/neurokinin (P/NK) receptor antago- tration/effect. May increase concentration/
nist. CLINICAL: Antinausea, antiemetic. effect of BCRP substrates (e.g., meth-
otrexate, rosuvastatin), CYP2D6
USES substrates (e.g., pimozide), P-gp
substrates (e.g., digoxin). HERBAL: St.
Prevention of delayed nausea and vom- John’s wort may decrease concentra-
iting associated with initial and repeat tion/effect. FOOD: None significant. LAB
courses of emetogenic cancer chemo- VALUES: May decrease Hct, Hgb, neutro-
therapy, including, but not limited to, phils, RBC.
highly emetogenic chemotherapy, in com-
bination with other antiemetic agents. AVAILABILITY (Rx)
PRECAUTIONS Emulsion, IV: 166.5 mg/92.5 ml. Tablets:
90 mg.
Contraindications: Hypersensitivity to
rolapitant. CYP2D6 substrates with a ADMINISTRATION/HANDLING
narrow therapeutic index (e.g., thiorida-
zine). Cautions: Mild to moderate hepatic IV
impairment, pts at risk for QT interval Rate of administration • Infuse over
prolongation or ventricular arrhyth- 30 minutes. Do not dilute. • Solution
mia (congenital long QT syndrome, is compatible with 0.9% NaCl, D5W or
medications that prolong QT interval, Lactated Ringers via Y-site.
R hypokalemia, hypomagnesemia). Not rec- Storage • Store at room temperature.
ommended in severe hepatic impairment.
PO
ACTION • Administer approx. 1–2 hrs prior to
Selectively and competitively inhibits human chemotherapy. • Give without regard to
substance P/NK1 receptors. Therapeutic food. Administer prior to initiation of
Effect: Decreases nausea and vomiting each chemotherapy cycle at no less than
associated with chemotherapy. 2-wk intervals.

PHARMACOKINETICS INDICATIONS/ROUTES/DOSAGE
Readily absorbed. Widely distributed. Chemotherapy-Associated Nausea/
Metabolized in liver. Protein binding: Vomiting
greater than 99%. Peak plasma concen- PO: ADULTS, ELDERLY: 180 mg once on day
tration: 4 hrs. Excreted in urine (14%), 1 (in combination with dexamethasone and
feces (73%). Half-life: 158 hrs. a 5-HT3 receptor antagonist). Do not give
rolapitant at intervals of less than 2 wks.
LIFESPAN CONSIDERATIONS IV: ADULTS, ELDERLY: 166.5 mg given within
Pregnancy/Lactation: Safety and effi- 2 hrs prior to initiation of chemotherapy on
cacy not established during pregnancy. day 1 (in combination with dexamethasone
Unknown if distributed in breast milk. and a 5-HT3 receptor antagonist).

underlined – top prescribed drug


romiDEPsin 1037
Dosage in Renal Impairment products. • Report persistent nausea,
Mild to moderate impairment: No vomiting despite treatment.
dose adjustment. Severe impairment:
Not specified; use caution.

Dosage in Hepatic Impairment romiDEPsin


Mild to moderate impairment: No
dose adjustment. Severe impairment: roe-mi-dep-sin
Treatment not recommended. (Istodax)
Do not confuse romiDEPsin with
SIDE EFFECTS romiPLOStim.
Occasional (9%–6%): Decreased appe-
uCLASSIFICATION
tite, hiccups, dizziness. Rare (4%–3%):
Abdominal pain. PHARMACOTHERAPEUTIC: Histone
deacetylase (HDAC) inhibitor. CLINICAL:
ADVERSE EFFECTS/TOXIC Antineoplastic.
REACTIONS
Torsades de pointes, QT prolongation USES
reported in pts taking thioridazine concom- Treatment of refractory cutaneous T-cell
itantly; avoid use. Baseline electrolyte imbal- lymphoma (CTCL) or refractory periph-
ance may increase risk of arrhythmias. eral T-cell lymphoma (PTCL).
NURSING CONSIDERATIONS PRECAUTIONS
BASELINE ASSESSMENT Contraindications: Hypersensitivity to romi-
Obtain CBC, BMP, serum magnesium. DEPsin. Cautions: Moderate or severe
Question history of arrhythmias, hepatic hepatic impairment, end-stage renal
impairment, congenital long QT syn- impairment, preexisting cardiac disease,
drome. Receive medication history and pts with QT interval prolongation, con-
screen for interactions. Assess hydration comitant administration of medications
status. Obtain ECG in pts taking concomi- prolonging QT interval, hypokalemia,
tant drugs that prolong QT interval. hypomagnesemia. Avoid concomitant
strong CYP3A4 inhibitors/inducers; cau- R
INTERVENTION/EVALUATION tion with moderate CYP3A4 inhibitors or
Periodically monitor CBC, BMP. Monitor P-glycoprotein inhibitors.
hydration, nutritional status, I&O. Correct
electrolyte imbalances prior to each dose. ACTION
If CYP2D6 substrate medications cannot be Catalyzes acetyl group removal from pro-
withheld, diligently monitor for QT interval tein lysine residues, resulting in acetyl
prolongation, ventricular arrhythmias. As- group accumulation, which alters chro-
sist with ambulation if dizziness occurs. As- matin structure and transcription fac-
sess for anemia-related symptoms. tor activation, terminating cell growth.
Therapeutic Effect: Induces cell-cycle
PATIENT/FAMILY TEACHING
arrest, cell death.
• Therapy may alter effectiveness of other
drugs. Do not take any newly prescribed PHARMACOKINETICS
medications unless approved by doctor Extensively metabolized. Protein binding:
who originally started treatment. • Re- 92%–94%. Half-life: 3 hrs.
port symptoms of arrhythmias such as
chest pain, dizziness, fainting, fatigue, pal- LIFESPAN CONSIDERATIONS
pitations, shortness of breath. • Do not Pregnancy/Lactation: May cause fetal
take herbal products or ingest grapefruit harm. Unknown if distributed in breast
Canadian trade name Non-Crushable Drug High Alert drug
1038 romiDEPsin
milk. Children: Safety and efficacy not days if pt continues to benefit from and
established. Elderly: No age-related tolerates therapy.
precautions noted.
Dose Modification
INTERACTIONS Hematologic Toxicity
DRUG: Strong CYP3A4 inhibitors Grade 3 or 4 neutropenia or throm-
(e.g., clarithromycin, itraconazole, bocytopenia: Delay treatment until
ritonavir) may increase concentration. ANC 1,500 cells/mm3 or more and/or
Strong CYP3A4 inducers (e.g., car- platelets 75,000 cells/mm3 or more (or
BAMazepine, phenytoin, rifAMPin) baseline), then resume at 14 mg/m2.
may decrease concentration. QT inter- Grade 4 neutropenia or thrombocy-
val–prolonging medications (e.g., topenia requiring platelet transfu-
amiodarone, azithromycin, ceri- sion: Delay treatment until recovered to
tinib, haloperidol, moxifloxacin) may Grade 1 or 0 (or baseline), then perma-
increase risk of QT interval prolongation, nently reduce dose to 10 mg/m2.
cardiac arrhythmias. May increase adverse Nonhematologic Toxicity (Excluding
effects; decrease therapeutic effect of vac- Alopecia)
cines (live). HERBAL: Echinacea may Grade 2 or 3 toxicity: Delay treatment
decrease therapeutic effect. FOOD: Grape- until recovered to Grade 1 or 0 ( or base-
fruit products may increase concentra- line); may restart at 14 mg/m2. Grade
tion/effects. LAB VALUES: May decrease 4, recurrent Grade 3 toxicity: Delay
Hgb, Hct, WBC count, platelets, serum treatment until recovered to Grade 1 or 0
magnesium, calcium, potassium, sodium, (or baseline), then permanently reduce
albumin, phosphates. May increase serum dose to 10 mg/m2. Recurrent Grade
glucose, ALT, AST, uric acid. May alter 3 or 4 toxicity (with dose reduc-
serum magnesium. tion): Permanently discontinue.

AVAILABILITY (Rx) Dosage in Renal Impairment


Injection, Powder for Reconstitution,
No dose adjustment. Use caution in end-
2-Vial Kit: 10 mg.
stage-renal disease.
Dosage in Hepatic Impairment
R ADMINISTRATION/HANDLING
Mild impairment: No dose adjustment.
Reconstitution • Reconstitute powder Moderate to severe impairment: Use
with 2 mL of supplied diluent (80% propylene caution.
glycol, 20% dehydrated alcohol). • Swirl
contents gently to dissolve powder. • Recon- SIDE EFFECTS
stituted solution provides 5 mg/mL. Further Frequent (57%–23%): Nausea, fatigue,
dilute in 500 mL 0.9% NaCl. vomiting, anorexia. Occasional (20%–
Rate of administration • Infuse over 7%): Diarrhea, fever, distorted sense of
4 hrs. taste, constipation, hypotension, pruri-
Storage • Reconstituted solution is tus. Rare (4%–2%): Dermatitis, T-wave
stable for at least 24 hrs at room tem- and ST-wave changes on ECG.
perature. • Solution appears clear, col-
orless. Discard if precipitate is present or ADVERSE EFFECTS/TOXIC
solution is discolored. REACTIONS
INDICATIONS/ROUTES/DOSAGE Infection (47% of pts), including sepsis,
arrhythmias, acute respiratory distress
CTCL, PTCL syndrome, acute renal failure. Anemia
IV: ADULTS, ELDERLY: 14 mg/m2 admin- occurs in 19% of pts, thrombocytopenia
istered over 4 hrs on days 1, 8, and 15 of in 17% of pts, neutropenia in 11% of pts.
a 28-day cycle. Repeat cycles every 28

underlined – top prescribed drug


romosozumab-aqqg 1039

NURSING CONSIDERATIONS uCLASSIFICATION


PHARMACOTHERAPEUTIC: Sclerostin
BASELINE ASSESSMENT inhibitor. Monoclonal antibody.
Provide emotional support. Baseline CLINICAL: Osteoporosis agent.
CBC, BMP, LFT, PT/INR, serum magne-
sium, ionized calcium; capillary blood
glucose; ECG should be obtained prior to USES
therapy at baseline and routinely thereaf- Treatment of postmenopausal women
ter. Inform women of childbearing poten- with osteoporosis at high risk for frac-
tial of risk to fetus if pregnancy occurs. ture, defined as history of osteoporotic
INTERVENTION/EVALUATION
fracture, multiple risk factors for frac-
ture, or pts who have failed or intolerant
Calculate daily absolute neutrophil count to other osteoporosis therapy.
(ANC). Closely monitor hematologic,
chemistry parameters, ECG. Diligently PRECAUTIONS
monitor for infection. Provide antiemet- Contraindications: Hypersensitivity to
ics to control nausea/vomiting. romosozumab-aqqg. Hypocalcemia
PATIENT/FAMILY TEACHING prior to initiation. Cautions: Severe
• Diarrhea may cause dehydration, elec- renal impairment (eGFR 15–29 mL/
trolyte depletion. • Do not have immuni- min) or receiving dialysis; pts at risk
zations without physician’s approval (low- for osteonecrosis of the jaw (cancer,
ers body’s resistance). • Avoid contact radiotherapy, poor oral hygiene, pre-
with those who recently received live virus existing dental disease or infection,
vaccine. • Avoid crowds, those with anemia, coagulopathy, recent dental
­infection. • May reduce effectiveness procedures, tooth extraction). History
of estrogen-containing contraceptives. of MI, CVA, cardiovascular disease.
• Report excessive nausea or vomiting, Avoid use in pts with recent (within
palpitations, chest pain, shortness of 1 yr) MI, CVA.
breath. Seek immediate medical attention ACTION
if unusual bleeding occurs.
Stimulates osteoblastic activity by inhib-
iting sclerostin, a regulatory factor in R
bone metabolism. Therapeutic Effect:
romosozumab-aqqg Increases bone mass, improves bone
structure and strength, decreases bone
roe-moe-soz-ue-mab reabsorption.
(Evenity)
j BLACK BOX ALERT jMay PHARMACOKINETICS
increase risk of myocardial infarc- Widely distributed. Degraded into small
tion (MI), cerebrovascular accident
(CVA), cardiovascular death. Do not peptides and amino acids via catabolic
initiate in pts with recent (within 1 pathway. Peak plasma concentration: 5
yr) MI, CVA. In pts with other car- days. Steady state reached in 3 mos. Half-
diovascular risks, consider whether life: 12.8 days.
the benefits of treatment outweigh
the risks. Discontinue treatment in LIFESPAN CONSIDERATIONS
pts who develop MI, CVA.
Do not confuse romosozumab Pregnancy/Lactation: Not indicated
with atezolizumab, mepolizum- in female pts of reproductive potential.
Children: Safety and efficacy not estab-
ab, pembrolizumab, trastuzum-
ab, or vedolizumab, or Evenity lished. Elderly: No age-related precau-
with Emgality. tions noted.

Canadian trade name Non-Crushable Drug High Alert drug


1040 romosozumab-aqqg

INTERACTIONS Dosage in Hepatic Impairment


Mild to severe impairment: Not speci-
DRUG: None significant. HERBAL: None
significant. FOOD: None known. LAB VAL- fied; use caution.
UES: May decrease calcium. SIDE EFFECTS
AVAILABILITY (Rx) Occasional (13%–6%): Arthralgia, head-
Injection Solution, Prefilled Syringe: 105 ache. Rare (4%–2%): Injection site reac-
mg/1.17 mL. tions (pain, erythema), muscle spasms,
peripheral edema, asthenia, neck pain,
ADMINISTRATION/HANDLING insomnia, paresthesia.
SQ ADVERSE EFFECTS/TOXIC
Preparation • Remove prefilled syringe REACTIONS
from refrigerator and allow solution to
warm to room temperature (at least 30 MI, CVA, cardiovascular death reported
min) with needle cap intact. • Visually in less than 1% of pts. Hypocalcemia re-
inspect for particulate matter or discol- ported in less than 1% of pts. Pts with
oration. Solution should appear clear to severe renal impairment (eGFR 15–29
opalescent, colorless to slightly yellow in mL/min) or receiving dialysis have an
color. Do not use if solution is cloudy or increased risk of hypocalcemia. Hyper-
discolored or if visible particles are sensitivity reactions including angio-
observed. edema, erythema multiforme, dermatitis,
Administration • Insert needle sub-
rash, urticaria may occur. Symptomatic
cutaneously into upper arm, outer thigh, hypocalcemia reported in 7% of pts. Os-
or abdomen and inject solution. • Do teonecrosis of the jaw may present as
not inject into areas of active skin disease mandibular pain, jaw bone erosion, peri-
or injury such as sunburns, skin rashes, odontal/gingival infection or ulceration,
inflammation, skin infections, or active osteomyelitis, slow healing of the mouth
psoriasis. • Rotate injection sites. after dental procedures. Pts with cancer,
• Do not administer IV or intramuscu- radiotherapy, poor oral hygiene, preex-
larly. • If a dose is missed, administer isting dental disease or infection, anemia,
as soon as possible, then give next dose coagulopathy may be at increased risk of
R at the date of last dose. developing osteonecrosis of the jaw.
Storage • Refrigerate prefilled syringes
Atypical subtrochanteric and diaphyseal
in original carton until time of femoral fractures may occur with little or
use. • Protect from light. • Do not no trauma. Immunogenicity (auto-romo-
shake. • Do not freeze or expose to sozumab antibodies) reported in 18% of
heating sources. • If not refrigerated, pts.
may store at room temperature (up to NURSING CONSIDERATIONS
77°F) for no more than 30 days. Discard
of not used within 30 days. BASELINE ASSESSMENT
Obtain serum calcium level. Hypocalce-
INDICATIONS/ROUTES/DOSAGE mia must be corrected prior to initiation.
Postmenopausal Osteoporosis Calcium and vitamin D supplementation
SQ: ADULTS, ELDERLY: 210 mg (two 105- is recommended during treatment. Ques-
mg injections) once monthly for 12 mos. tion history of MI, CVA, cardiovascular
Give with supplemental calcium and vita- disease, renal impairment. Do not initi-
min D. ate in pts with recent (within 1 yr) MI,
CVA. To assess the risk of osteonecrosis
Dosage in Renal Impairment of the jaw, the prescriber should perform
Mild to severe impairment: No dose an oral examination prior to initiation.
adjustment.
underlined – top prescribed drug
rOPINIRole 1041
Question recent dental procedures or uCLASSIFICATION
tooth extraction. PHARMACOTHERAPEUTIC: DOPamine
INTERVENTION/EVALUATION agonist. CLINICAL: Antiparkinson agent.
Monitor serum calcium levels periodi-
cally, esp. in pts with severe renal im- USES
pairment or receiving dialysis. Monitor Treatment of signs/symptoms of idiopathic
for symptoms of CVA (aphasia, altered Parkinson’s disease. Immediate-Release
mental status, headache, hemiplegia, vi- Only: Treatment of moderate to severe pri-
sion loss); MI (chest pain, dyspnea, syn- mary restless legs syndrome (RLS).
cope, diaphoresis, arm/jaw pain), osteo-
necrosis of the jaw (jaw pain/numbness, PRECAUTIONS
loosening of teeth, poor healing of the Contraindications: Hypersensitivity to
gums; hypocalcemia (muscle spasm, my- rOPINIRole. Cautions: History of ortho-
algia, paresthesia, seizures, QT interval static hypotension, cardiovascular or
prolongation, ventricular arrhythmias; cerebrovascular disease, syncope, hallu-
Chvostek’s sign, Trousseau’s sign). A cinations (esp. in elderly pts), concurrent
dull, aching thigh or groin pain should be use of CNS depressants, preexisting dyski-
evaluated for possible femoral fractures. nesia, hepatic or severe renal dysfunction
Monitor for hypersensitivity reactions. (end-stage renal disease [ESRD]), major
PATIENT/FAMILY TEACHING psychotic disorder, elderly pts.
• Report symptoms of heart attack (chest ACTION
pain, difficulty breathing, jaw pain, nau- Stimulates postsynaptic DOPamine recep­
sea, pain that radiates to the arm or jaw, tors in caudate putamen in the brain.
sweating), stroke (confusion, one-sided Therapeutic Effect: Relieves signs/
weakness, loss of consciousness, trouble symptoms of Parkinson’s disease.
speaking, vision loss); atypical leg frac-
tures (dull, aching thigh or groin pain). PHARMACOKINETICS
• Treatment may cause low blood cal- Rapidly absorbed after PO administration.
cium levels; report difficulty swallowing, Protein binding: 40%. Widely distributed.
fatigue, muscle cramps, muscle weak- Extensively metabolized. Steady-state R
ness, palpations, paralysis, numbness, concentrations achieved within 2 days.
tingling, seizures. • Treatment may cause Excreted in urine. Unknown if removed
lack of blood supply to the jaw bone by hemodialysis. Half-life: 6 hrs.
when the bone is exposed, which may
lead to jaw necrosis. Report jaw pain or LIFESPAN CONSIDERATIONS
numbness, loosening of teeth, poor heal- Pregnancy/Lactation: Distributed
ing of the gums. Maintain proper oral in breast milk. Drug activity possible in
hygiene. • Allergic reactions such as breastfeeding infant. Children: Safety
swelling of the face or tongue, rash, itch- and efficacy not established. Elderly: No
ing may occur. age-related precautions noted, but halluci-
nations may occur more frequently.
INTERACTIONS
rOPINIRole DRUG: Ciprofloxacin may increase
concentration. Alcohol, CNS depres-
roe-pin-i-role sants (e.g., LORazepam, morphine,
(Requip, Requip XL) zolpidem) may increase CNS depressant
Do not confuse rOPINIRole with effects. Antipsychotic agents (e.g.,
RisperDAL or risperiDONE. haloperidol) may decrease therapeutic

Canadian trade name Non-Crushable Drug High Alert drug


1042 rOPINIRole
effect. HERBAL: Herbals with hypoten- until reaching daily dose of 3 mg during wk
sive properties (e.g., garlic, ginger, 6. Daily dose may be increased to maximum
gingko biloba) may increase hypoten- of 4 mg beginning wk 7. Give all doses 1–3
sive effect. FOOD: All foods delay peak hrs before bedtime. ESRD: 3 mg maximum.
plasma levels by 1 hr but do not affect
Dosage in Renal/Hepatic Impairment
drug absorption. LAB VALUES: May
increase serum alkaline phosphatase. No dose adjustment. Use caution with
severe renal impairment. Titrate cau-
AVAILABILITY (Rx) tiously in pts with hepatic impairment.
Tablets:0.25 mg, 0.5 mg, 1 mg, 2 mg, 3 mg, SIDE EFFECTS
4 mg, 5 mg. Frequent (60%–40%): Nausea, dizziness,
Tablets, Extended-Release: 2 mg, 4 mg, extreme drowsiness. Occasional (12%–
6 mg, 8 mg, 12 mg. 5%): Syncope, vomiting, fatigue, viral
infection, dyspepsia, diaphoresis, asthe-
ADMINISTRATION/HANDLING nia, orthostatic hypotension, abdominal
PO discomfort, pharyngitis, abnormal vision,
• May give without regard to food. • Do dry mouth, hypertension, hallucinations,
not break, crush, dissolve, or divide confusion. Rare (Less Than 4%): Anorexia,
extended-release tablets. peripheral edema, memory loss, rhinitis,
sinusitis, palpitations, impotence.
INDICATIONS/ROUTES/DOSAGE
Parkinson’s Disease ADVERSE EFFECTS/TOXIC
PO: (Immediate-Release): ADULTS, REACTIONS
ELDERLY: Initially, 0.25 mg 3 times/day. Dyskinesia, impulsive/compulsive behav-
Based on individual pt response, dosage ior (pathologic gambling, hypersexuality,
should be titrated with wkly increments. Wk binge-eating) occur rarely.
1: 0.25 mg 3 times/day; total daily dose:
0.75 mg. Wk 2: 0.5 mg 3 times/day; total NURSING CONSIDERATIONS
daily dose: 1.5 mg. Wk 3: 0.75 mg 3 times/
day; total daily dose: 2.25 mg. Wk 4: 1 mg BASELINE ASSESSMENT
3 times/day; total daily dose: 3 mg. After Parkinson’s disease: Assess signs/
R wk 4: May increase dose by 1.5 mg/day on symptoms (e.g., tremor, gait). Restless
wkly basis up to dose of 9 mg/day. May then legs syndrome: Assess frequency of
further increase by 3 mg/day on wkly basis symptoms, sleep pattern.
up to total dose of 24 mg/day (ESRD: 18
mg). (Extended-Release): Initially, 2 mg INTERVENTION/EVALUATION
once daily for 1–2 wks. May increase by 2 Assess for clinical improvement, clinical
mg/day at 1 wk or longer interval. Maxi- reversal of symptoms (improvement of
mum: 24 mg/day. ESRD: 18 mg. tremors of head/hands at rest, mask-like
Discontinuation Taper
facial expression, shuffling gait, muscular
Gradually taper over 7 days as follows: rigidity). Assist with ambulation if dizziness
Decrease frequency from 3 times/day to occurs. Monitor B/P, daytime alertness.
twice daily for 4 days, then decrease from PATIENT/FAMILY TEACHING
twice daily to once daily for remaining 3 days. • Drowsiness, dizziness may be an initial
Restless Legs Syndrome response to drug. • Postural hypoten-
PO: (Immediate-Release): ADULTS, sion may occur more frequently during
ELDERLY: 0.25 mg once daily for days 1 and initial therapy. Slowly go from lying to
2. May increase to 0.5 mg daily for days 3–7 standing. • Avoid tasks that require
and after 7 days to 1 mg daily. May further alertness, motor skills until response to
titrate upward in 0.5-mg increments q7days drug is established. • If nausea occurs,

underlined – top prescribed drug


rosuvastatin 1043
take medication with food. • Hallucina- impairment, acute renal failure, uncon-
tions may occur, more so in the elderly trolled hypothyroidism, elderly pts.
than in younger pts with Parkinson’s dis-
ease. • Report occurrence of falling ACTION
asleep during activities of daily living, new Interferes with cholesterol biosynthesis by
or worsening symptoms, changes in B/P, inhibiting conversion of the enzyme HMG-
fainting, unusual urges. • Avoid alcohol. CoA to mevalonate, a precursor to choles-
terol. Therapeutic Effect: Decreases
LDL, VLDL, plasma triglyceride levels;
rosuvastatin increases HDL concentration.
PHARMACOKINETICS
roe-soo-va-sta-tin Protein binding: 88%. Minimal hepatic
(Apo-Rosuvastatin , Crestor) metabolism. Primarily excreted in feces.
Do not confuse rosuvastatin with Half-life: 19 hrs (increased in severe renal
atorvastatin, lovastatin, nystatin, dysfunction).
pitavastatin, or simvastatin.
LIFESPAN CONSIDERATIONS
uCLASSIFICATION
Pregnancy/Lactation: Contraindi-
PHARMACOTHERAPEUTIC: HMG-CoA cated in pregnancy (suppression of
reductase inhibitor. CLINICAL: Anti- cholesterol biosynthesis may cause
hyperlipidemic. fetal toxicity), lactation. Risk of seri-
ous adverse reactions in breastfeeding
infants. Children: Safety and efficacy
USES
not established in children younger than
Adjunct to diet therapy in pts with primary 7 yrs. Elderly: No age-related precau-
hyperlipidemia and mixed dyslipidemia; tions noted.
to decrease elevated total, LDL choles-
terol, serum triglyceride levels; increases INTERACTIONS
HDL. Adjunct to diet to slow progression DRUG: Aluminum- and magnesium-
of atherosclerosis in pts with elevated containing antacids may decrease
cholesterol. Treatment of primary dysbet- concentration/effects. Increased risk R
alipoproteinemia, homozygous familial of myopathy with colchicine, cyclo-
hypercholesterolemia (HoFH). Treatment SPORINE, fenofibrate, fenofibrate
of pts ages 10–17 yrs with heterozygous derivatives, gemfibrozil, niacin.
familial hypercholesterolemia (HeFH) to May increase anticoagulant effect of
reduce elevated total cholesterol, LDL cho- warfarin. HERBAL: None significant.
lesterol, and apolipoprotein B. Primary FOOD: Red yeast rice contains 2.4
prevention of cardiovascular disease (risk mg lovastatin per 600 mg rice. LAB
reduction of MI, stroke, arterial revascu- VALUES: May increase serum alkaline
larization) without clinically evident CAD, phosphatase, bilirubin, creatinine phos-
but with multiple risk factors. phokinase, glucose, transaminases. May
produce hematuria, proteinuria.
PRECAUTIONS
Contraindications: Hypersensitivity to AVAILABILITY (Rx)
ro­
suvastatin. Active hepatic disease, Tablets: 5 mg, 10 mg, 20 mg, 40 mg.
breastfeeding, pregnancy, unexplained,
persistent elevations of hepatic enzymes. ADMINISTRATION/HANDLING
Cautions: Anticoagulant therapy, hepatic PO
impairment, substantial alcohol con- • Give without regard to food. May give
sumption, elective major surgery, renal at any time of day.

Canadian trade name Non-Crushable Drug High Alert drug


1044 rucaparib

INDICATIONS/ROUTES/DOSAGE ADVERSE EFFECTS/TOXIC


Hyperlipidemia, Dyslipidemia, REACTIONS
Atherosclerosis, Dysbetalipoproteinemia, Potential for ocular lens opacities. Hyper-
Primary Prevention of Cardiovascular sensitivity reaction, hepatitis, rhabdomy-
Disease olysis occur rarely.
PO: ADULTS, ELDERLY: Usual starting
dosage is 10–20 mg/day, with adjust- NURSING CONSIDERATIONS
ments based on lipid levels; monitor BASELINE ASSESSMENT
q2–4wks until desired level is achieved.
Lower starting dose of 5 mg is recom- Obtain dietary history, esp. fat consump-
mended in pts of Asian ancestry. Maxi- tion. Question for possibility of preg-
mum: 40 mg/day. Range: 5–40 mg/day. nancy. Assess baseline lab results: serum
cholesterol, triglycerides, LFT.
HoFH
INTERVENTION/EVALUATION
PO: ADULTS, ELDERLY: Initially, 20 mg/
day. Range: 5–40 mg/day. Maxi- Monitor serum cholesterol, HDL, LDL, tri-
mum: 40 mg/day. CHILDREN 7 YRS AND glycerides for therapeutic response. Lipid
OLDER: 20 mg once daily. levels should be monitored within 2–4 wks
of initiation of therapy or change in dosage.
HeFH Monitor LFT at 12 wks following initiation
PO: CHILDREN 10–17 YRS: Initially, 20 mg of therapy, at any elevation of dose, and
once daily. Range: 5–20 mg once daily. periodically (e.g., semiannually) thereafter.
Maximum: 20 mg. 8–9 YRS: 5–10 mg Monitor CPK if myopathy is suspected. Mon-
once daily. Maximum: 10 mg. itor daily pattern of bowel activity, stool con-
sistency. Assess for headache, sore throat.
Concurrent CycloSPORINE Use Be alert for myalgia, weakness.
PO: ADULTS, ELDERLY: 5 mg/day maximum.
PATIENT/FAMILY TEACHING
Concurrent Gemfibrozil, Atazanavir/
• Use appropriate contraceptive mea-
Ritonavir, Lopinavir/Ritonavir or
sures. • Periodic lab tests are essential part
Simeprevir Therapy
of therapy. • Maintain appropriate diet
PO: ADULTS, ELDERLY: Initially, 5 mg/ (important part of treatment). • Report
R day. 10 mg/day maximum. unexplained muscle pain, tenderness, weak-
Dosage in Renal Impairment (CrCl Less ness, esp. if associated with fever, malaise.
Than 30 mL/min)
PO: ADULTS, ELDERLY: 5 mg/day; do not
exceed 10 mg/day.
rucaparib
Dosage in Hepatic Impairment
Contraindicated in active in liver disease. roo-kap-a-rib
(Rubraca)
SIDE EFFECTS Do not confuse rucaparib with
Generally well tolerated. Side effects are neratinib, niraparib, olaparib.
usually mild, transient. Occasional (9%–
uCLASSIFICATION
3%): Pharyngitis, headache, diarrhea, dys-
pepsia, nausea, depression. Rare (Less Than PHARMACOTHERAPEUTIC: Poly (ADP-­
3%): Myalgia, asthenia, back pain. ribose) polymerase (PARP) inhibi-
tor. CLINICAL: Antineoplastic.

underlined – top prescribed drug


rucaparib 1045

USES VALUES: May increase serum ALT, AST,


Treatment of deleterious germline and/ cholesterol, creatinine. May decrease
or somatic BRCA mutation–associated ANC, Hgb, absolute lymphocyte count,
(detected by FDA-approved test) platelets.
advanced ovarian cancer in pts who have AVAILABILITY (Rx)
been treated with two or more lines of
Tablets: 200 mg, 250 mg, 300 mg.
chemotherapy. Maintenance treatment
of recurrent ovarian cancer in pts who ADMINISTRATION/HANDLING
are in complete or partial response to PO
platinum-based chemotherapy. • Give with or without food. • If a dose
PRECAUTIONS is missed or vomiting occurs after admin-
istration, do not give extra dose. Adminis-
Contraindications: Hypersensitivity to ter next dose at regularly scheduled time.
rucaparib. Cautions: Baseline hemato-
logic cytopenias (anemia, neutropenia, INDICATIONS/ROUTES/DOSAGE
thrombocytopenia, lymphocytopenia). Note: Administer only to pts with del-
eterious germline and/or somatic BRCA
ACTION mutation.
Inhibits poly (ADP-ribose) polymerase
Ovarian Cancer (Advanced or
(PARP) enzymes (involved in DNA tran-
Maintenance of Recurrent)
scription, cell-cycle regulation, and DNA
PO: ADULTS, ELDERLY: 600 mg twice daily
repair). By inhibiting PARP, may cause
PARP DNA complexes resulting in DNA about 12 hrs apart. Continue until disease
damage and cellular death. Therapeutic progression or unacceptable toxicity.
Effect: Inhibits tumor cell growth and Dose Reduction Schedule
metastasis. Starting dose: 600 mg twice daily.
First dose reduction: 500 mg twice
PHARMACOKINETICS daily. Second dose reduction: 400
Widely distributed. Metabolized in liver. mg twice daily. Third dose reduction:
Protein binding: 70%. Peak plasma con- 300 mg twice daily.
centration: 1.9 hrs. Excretion not speci-
fied. Half-life: 17–19 hrs. Dose Modification R
Adverse Events, Non-Hematologic
LIFESPAN CONSIDERATIONS Toxicity
Pregnancy/Lactation: Avoid pregna­ncy; Either withhold treatment or reduce dos-
may cause fetal harm. Females of reproduc- age per dose reduction schedule.
Hematologic Toxicity
tive potential should use effective contracep-
tion during treatment and up to 6 mos after Withhold treatment until improved to
discontinuation. Unknown if distributed CTCAE Grade 1 or 0 and investigate cause.
in breast milk. Breastfeeding not recom- If myelodysplastic syndrome or acute
mended during treatment and for at least 2 myeloid leukemia confirmed, permanently
wks after discontinuation. Children: Safety discontinue.
and efficacy not established. Elderly: No Dosage in Renal Impairment
age-related precautions noted. Mild to moderate impairment: No
dose adjustment. Severe impairment,
INTERACTIONS ESRD: Not specified; use caution.
DRUG: May decrease effect of BCG vac-
cine. May increase concentration/effect Dosage in Hepatic Impairment
of cilostazol, lomitapide, pimozide, Mild impairment: No dose adjust-
rasagiline, tiZANidine. HERBAL: None ment. Moderate to severe impair-
significant. FOOD: None known. LAB ment: Not specified; use caution.

Canadian trade name Non-Crushable Drug High Alert drug


1046 rufinamide

SIDE EFFECTS PATIENT/FAMILY TEACHING


Frequent (77%–21%): Nausea, asthenia, • Treatment may depress your immune
fatigue, vomiting, constipation, dysgeusia, system response and reduce your abil-
decreased appetite, diarrhea, abdominal ity to fight infection. Report symptoms
pain, dyspnea. Occasional (17%–9%): Diz- of infection such as body aches, chills,
ziness, rash, pyrexia, photosensitivity reac- cough, fatigue, fever. Avoid those with ac-
tion, pruritus. tive infection. • Report bleeding or easy
bruising, bloody urine or stool, frequent
ADVERSE EFFECTS/TOXIC infections, fatigue, shortness of breath,
REACTIONS weakness, weight loss; may indicate acute
Anemia, lymphopenia, neutropenia, throm- bone marrow depression or acute leuke-
bocytopenia are expected responses to mia. • Avoid pregnancy; treatment may
therapy. Myelodysplastic syndrome/acute cause birth defects. Females of childbear-
myeloid leukemia reported in less than ing potential should use effective contra-
1% of pts. Infections including nasophar- ception during treatment and for at least 6
yngitis, pharyngitis, upper respiratory tract mos after last dose. • Do not breastfeed
infection occurred in 43% of pts. Febrile during treatment and for at least 2 wks after
neutropenia reported in less than 1% of final dose. • Do not take herbal supple-
pts. Palmar-plantar erythrodysesthesia syn- ments. • Report planned surgical/dental
drome (PPES), a chemotherapy-induced procedures.
skin condition, that presents with redness,
swelling, numbness, skin sloughing of the
hands and feet, was reported in 2% of pts.
rufinamide
NURSING CONSIDERATIONS rue-fin-a-myde
(Banzel)
BASELINE ASSESSMENT
uCLASSIFICATION
Obtain baseline CBC, vital signs, weight. Do
not initiate therapy until pts have recovered PHARMACOTHERAPEUTIC: Triazole
from hematologic toxicities caused by pre- derivative. CLINICAL: Anticonvulsant.
vious chemotherapy. Obtain pregnancy test
R in females of reproductive potential. Ques- USES
tion plans of breastfeeding. Question history
of hepatic/renal impairment, hypercholes- Adjunctive therapy in treatment of seizures
terolemia. Screen for risk of bleeding, ac- associated with Lennox-Gastaut syndrome
tive infection. Offer emotional support. in adults and children 1 yr and older.

INTERVENTION/EVALUATION PRECAUTIONS
Monitor CBC monthly; serum cholesterol, Contraindications: Hypersensitivity to rufin­
creatinine periodically. For prolonged amide. Familial short QT syndrome.
hematologic toxicities caused by other Cautions: Other drugs that shorten QT
chemotherapies, monitor CBC wkly until interval, clinical depression, pts at high
recovery. If hematologic levels have not risk for suicide, mild to moderate hepatic
recovered to CTCAE Grade 1 or 0 after 4 impairment (not recommended in pts
wks, consider hematology consultation with severe hepatic impairment), concur-
for further investigations including bone rent use with hormonal contraceptives.
marrow analysis, blood sample for cyto-
genetics. Diligently monitor for infection. ACTION
Monitor for myelodysplastic syndrome, Modulates activity of sodium channels.
acute myeloid leukemia. Assess skin for Prolongs inactive state of the sodium chan-
rash, lesions, sloughing. Monitor for de- nel in cortical neurons, limits sustained
creased urine output, renal dysfunction. repetitive firing of sodium-dependent
underlined – top prescribed drug
rufinamide 1047
action potential, inhibiting excitatory mg/day every 2 days. Maximum: 3,200
neurotransmitter release. Therapeutic mg/day, administered in 2 equally divided
Effect: Decreases frequency/severity of doses. CHILDREN 1 YR AND OLDER: Treat-
seizure activity. ment should be initiated at a daily dose of
10 mg/kg/day, given in 2 equally divided
PHARMACOKINETICS doses. Increase by 10-mg/kg increments
Well absorbed following PO administra- every other day to a target dose of 45 mg/
tion. Protein binding: 34%. Extensively kg/day or 3,200 mg/day, whichever is less,
metabolized via hydrolysis. Excreted pri- administered in 2 equally divided doses.
marily in urine. Half-life: 6–10 hrs.
Dosage in Renal Impairment
LIFESPAN CONSIDERATIONS No dose adjustment.
Pregnancy/Lactation: May produce
Dosage in Hepatic Impairment
fetal skeletal abnormalities. May be distrib-
uted in breast milk. Children: Safety and Mild to moderate impairment: Use
efficacy not established in pts younger than caution. Severe impairment: Not
4 yrs. Elderly: Age-related renal, hepatic, reco­m­mended.
or cardiac impairment may require initia- SIDE EFFECTS
tion of therapy at low end of dosing range.
Children: Frequent (27%–11%): Head-
INTERACTIONS ache, dizziness, fatigue, nausea,
DRUG: May increase concentration of drowsiness, diplopia. Occasional (6%–
4%): Tremor, nystagmus, blurred vision,
PHENobarbital, phenytoin. May
decrease concentration of carBAMaze- vomiting. Rare (3%): Ataxia, upper abdom-
pine. Valproate may increase concentra- inal pain, anxiety, constipation, dyspep-
tion. Alcohol, CNS depressants (e.g., sia, back pain, gait disturbance, vertigo.
LORazepam, morphine, zolpidem) may Adults: Frequent (17%–7%): Lethargy,
increase CNS depressant effect. HERBAL: vomiting, headache, fatigue, dizziness,
None significant. FOOD: None known. LAB nausea. Occasional (5%–4%): Influenza,
VALUES: May decrease WBC count.
nasopharyngitis, anorexia, rash, ataxia,
diplopia. Rare (3%): Bronchitis, sinus-
AVAILABILITY (Rx) itis, psychomotor hyperactivity, upper R
Oral Suspension: 40 mg/mL. Tablets,
abdominal pain, aggression, ear infec-
Film-Coated: 200 mg, 400 mg.
tion, inattention, pruritus.

ADMINISTRATION/HANDLING ADVERSE EFFECTS/TOXIC


REACTIONS
PO
• Give with food. • Film-coated tablets Suicidal ideation or behavior occurs rarely,
may be cut or crushed for dosing flexibil- noted as early as 1 wk after initiation of ther-
ity. • Shake oral suspension well before apy and persisting for at least 24 wks. Short-
each dose; use bottle adapter and dosing ening of the QT interval (up to 20 msec),
syringes provided. hypersensitivity reaction (rash, fever, urti-
caria) have been noted. Abrupt withdrawal
INDICATIONS/ROUTES/DOSAGE may precipitate seizure, status epilepticus.
Lennox-Gastaut Seizures NURSING CONSIDERATIONS
Note: Discontinue therapy gradually to
minimize potential of increased seizure BASELINE ASSESSMENT
frequency (e.g., decrease by 25% q2days). Review history of seizure disorder (in-
PO: ADULTS, ELDERLY: Initially, 400–800 tensity, frequency, duration, level of con-
mg/day, given in 2 equally divided doses. sciousness). Obtain baseline ECG. Initiate
Dose should be increased by 400–800 seizure precautions.
Canadian trade name Non-Crushable Drug High Alert drug
1048 ruxolitinib
INTERVENTION/EVALUATION use of strong CYP3A4 inhibitors, history
Provide safety measures as needed. Observe of bradycardia, conduction disturbances,
frequently for recurrence of seizure activity. ischemic heart disease, HF.
Assess for clinical improvement (decrease
in intensity, frequency of seizures). Assist ACTION
with ambulation if drowsiness, lethargy oc- Inhibits Janus-associated kinases (JAKs)
cur. Question for evidence of headache. JAK1 and JAK2, which mediates the
signaling of cytokines and growth fac-
PATIENT/FAMILY TEACHING tor important for hematopoiesis and
• Do not abruptly withdraw medication immune function. In myelofibrosis and
(may precipitate seizures). • Avoid tasks polycythemia vera JAK1/2 activity is dys-
that require alertness, motor skills until regulated. Therapeutic Effect: Modu-
response to drug is established. • Strict lates the affected JAK1/2 activity.
maintenance of drug therapy is essential for
seizure control. • Avoid alcohol. • Fe- PHARMACOKINETICS
male pts of childbearing age should be Rapidly absorbed after PO administration.
informed that concurrent use of rufinamide Widely distributed. Protein binding: 97%.
with hormonal contraceptives may render Metabolized in liver. Excreted in urine
contraceptive less effective; nonhormonal (74%), feces (22%). Half-life: 3–5 hrs.
forms of contraception are recom-
mended. • Be alert for any unusual LIFESPAN CONSIDERATIONS
changes in mood/behavior (may increase Pregnancy/Lactation: Unknown if
risk of suicidal ideation/behavior). dist­ributed in breast milk. Not recom-
mended in nursing mothers. Must either
discontinue drug or discontinue breast-
ruxolitinib feeding. Children: Safety and efficacy
not established. Elderly: No age-related
rux-oh-li-ti-nib precautions noted.
(Jakafi)
INTERACTIONS
uCLASSIFICATION
DRUG: Strong CYP3A4 inhibitors (e.g.,
R PHARMACOTHERAPEUTIC: Janus-asso­ clarithromycin, ketoconazole) may
ciated tyrosine kinase inhibitor. CLINI- increase concentration/effects. May
CAL: Antineoplastic. increase adverse effects; decrease
therapeutic effect of vaccines (live).
HERBAL: None known. FOOD: Grapefruit
USES
products may increase concentration.
Treatment of intermediate or high-risk LAB VALUES: May decrease platelets,
myelofibrosis, including primary myelo- RBC, Hgb, Hct, WBC. May increase serum
fibrosis, post–polycythemia vera myelofi- bilirubin, ALT, AST, cholesterol.
brosis, post–essential thrombocythemia
myelofibrosis. Treatment of polycythemia AVAILABILITY (Rx)
vera. Treatment of steroid-refractory acute Tablets: 5 mg, 10 mg, 15 mg, 20 mg, 25 mg.
graft-versus-host disease (GVHD) in adults
and children 12 yrs and older. ADMINISTRATION/HANDLING
PO
PRECAUTIONS
• Give without regard to food.
Contraindications: Hypersensitivity to rux­
olitinib. Cautions:Pts at risk for develop- Feeding Tube
ing bacterial, fungal, or viral infections, • Suspend tablet in 40 mL water and stir
renal/hepatic impairment, concomitant for 10 min. • May administer suspen­sion

underlined – top prescribed drug


ruxolitinib 1049
within 6 hrs after tablet has dis- SIDE EFFECTS
persed. • Flush with 75 mL water after Frequent (23%–14%): Bruising, dizziness,
administration. vertigo, labyrinthitis, headache. Occa-
sional (9%–7%): Weight gain, flatulence.
INDICATIONS/ROUTES/DOSAGE
Myelofibrosis ADVERSE EFFECTS/TOXIC
PO: ADULTS: 20 mg twice daily if plate- REACTIONS
lets greater than 200,000 cells/mm3, or May cause severe thrombocytopenia (70%
15 mg twice daily if platelets 100,000– of pts), anemia (96% of pts), neutropenia
200,000 cells/mm3, or 5 mg twice daily if (18% of pts), which may improve with
platelets 50,000 to less than 100,000 cells/ reduced dose or by temporarily withhold-
mm3. Dose reduction based on platelet ing regimen. Anemic pts may require blood
response. Maximum: 25 mg twice daily. transfusions. Increased risk of developing
Polycythemia Vera opportunistic bacterial, mycobacterial,
PO: ADULTS, ELDERLY: Initially, 10 mg fungal, viral infections including herpes
bid. Doses titrated based on safety/efficacy. zoster, urinary tract infection, urosepsis,
renal infection, pyuria. Increased risk of
GVHD
bleeding disorders including ecchymosis,
PO: ADULTS, ELDERLY, CHILDREN 12 YRS
hematoma, injection site hematoma, peri-
AND OLDER: Initially, 5 mg twice daily. May orbital hematoma, petechiae, purpura.
increase to 10 mg twice daily after at least 3
days (if ANC and platelets have not decreased NURSING CONSIDERATIONS
by 50% or greater from baseline).
BASELINE ASSESSMENT
Dosage in Renal/Hepatic Impairment Obtain CBC, serum chemistries, renal
Initial dose 10 mg bid. function, LFT, urinalysis, cholesterol level.
Dosage in Renal Impairment Assess recent vaccinations status. Receive
full medication history including herbal
CrCl 15–59 Platelets 10 mg twice products. Question for possibility of preg-
mL/min 100,000– daily nancy, renal/hepatic impairment, HIV.
150,000/mm 3

CrCl 15–59 Platelets less Avoid use INTERVENTION/EVALUATION


mL/min than R
100,000/mm3
Monitor CBC (every 2–4 wks until doses
End-stage Platelets 15 mg after stabilized), serum chemistries, renal
renal 100,000– dialysis on function, LFT, cholesterol. Obtain urinal-
disease 3
200,000/mm days of di- ysis with reflex culture for suspected UTI.
(ESRD) on alysis Routinely assess vital signs, I&O, breath
dialysis sounds, gait. Monitor temperature; be
ESRD on Platelets 20 mg after alert for fever, infectious process. Avoid
dialysis greater dialysis on IM injections, rectal temperatures, other
than days of di-
3
200,000/mm alysis
traumas that induce bleeding. Assess skin
ESRD not Avoid use for petechiae, hematoma, purpura.
requiring PATIENT/FAMILY TEACHING
dialysis
• Report any new bruising/bleeding, bloody
Dosage in Hepatic Impairment stools or urine, fever, chills, rash, painful
Hepatic Platelets 10 mg urination, suspected infection, fatigue, short-
impairment 100,000– twice ness of breath. • Do not breastfeed. • Avoid
150,000/mm 3 daily grapefruit products. • Open skin lesions,
Hepatic im- Platelets less Avoid use blisters may signal herpes infection. • Blood
pairment than work will be routinely monitored; if on dialy-
100,000/mm3 sis, take only following dialysis.
Canadian trade name Non-Crushable Drug High Alert drug
1050 sacubitril-valsartan

pts with chronic HF; produces vasodila-


sacubitril-valsartan tion; decreases peripheral resistance;
decreases B/P.
sak-ue-bi-tril
(Entresto) PHARMACOKINETICS
j BLACK BOX ALERT j May Widely distributed. Sacubitril is converted
cause fetal harm, mortality. by esterases; not significantly metabolized
Discontinue as soon as pregnancy after conversion. Valsartan is minimally
detected.
metabolized in liver. Protein binding
uCLASSIFICATION (both): 94%–97%. Peak plasma concen-
tration: sacubitril: 30 min, valsartan: 1.5
PHARMACOTHERAPEUTIC: Combina-
hrs. Steady-state concentration: 3 days.
tion of sacubitril, a neprilysin inhibi-
Excretion: sacubitril: urine (52%–68%),
tor, and valsartan, an angiotensin II
feces (37%–48%); valsartan: feces
receptor blocker. CLINICAL: Reduces
(86%), urine (13%). Half-life: sacubi-
risk of complications in HF.
tril: 1.4 hrs; valsartan: 9.9 hrs.
LIFESPAN CONSIDERATIONS
USES
Pregnancy/Lactation: Avoid preg-
To reduce the risk of cardiovascular nancy; may cause fetal harm/mortality.
death and hospitalization in pts with Unknown if distributed in breast milk.
chronic HF (NYHA class II-IV) and Must either discontinue drug or discon-
reduced ejection fraction. tinue breastfeeding. Children: Safety
PRECAUTIONS and efficacy not established. Elderly: No
age-related precautions noted.
Contraindications: Hypersensitivity to
sacubitril or valsartan; history of angio- INTERACTIONS
edema related to angiotensin-converting DRUG: ACE inhibitors (e.g., enala-
enzyme (ACE) inhibitor or angiotensin pril, ramipril) may increase risk of
receptor blockers (ARB); concomitant angioedema (contraindicated). Potas-
use or within 36 hrs of ACE inhibitors; sium-sparing diuretics (e.g., spi­
concomitant use of aliskiren in pts with rono­lactone) may increase risk of
diabetes. Cautions: Baseline anemia, hyperkalemia. NSAIDs (e.g., ibupro-
S dehydration, hypovolemia, sodium deple- fen, naproxen) may worsen renal func-
tion; concomitant use of potassium-spar- tion. May increase concentration/effect of
ing diuretics or potassium supplements; lithium. HERBAL: Herbals with hyper-
hepatic/renal impairment; unstented tensive properties (e.g., licorice,
bilateral/unilateral renal artery stenosis; yohimbe) or hypotensive properties
significant aortic/mitral stenosis. Pts with (e.g., garlic, ginger, ginkgo biloba)
orthostatic hypotension. may alter effects. FOOD: None known. LAB
VALUES: May increase serum BUN, creati-
ACTION nine, potassium. May decrease Hct, Hgb.
Sacubitril inhibits neprilysin, increas-
ing peptide levels that are degraded by AVAILABILITY (Rx)
neprilysin (e.g., natriuretic peptides). Fixed-Dose Combination Tablets: (Sacu-
Valsartan directly antagonizes angioten- bitril/valsartan): 24 mg/26 mg, 49 mg/51
sin II receptors; blocks vasoconstrictor, mg, 97 mg/103 mg.
aldosterone secreting effects of angio-
tensin II, inhibiting binding of angio- ADMINISTRATION/HANDLING
tensin II to AT1 receptors. Therapeutic PO
Effect: Decreases risk of mortality in • Give without regard to food.

underlined – top prescribed drug


sacubitril-valsartan 1051

INDICATIONS/ROUTES/DOSAGE
NURSING CONSIDERATIONS
HF
Note: Allow a 36-hr washout period when BASELINE ASSESSMENT
switching from or to an ACE inhibitor. After Obtain baseline BMP; CBC in pts with
initial dose, may double dose as tolerated baseline anemia. Obtain B/P, heart rate
q2–4wks to target dose of 97 mg/103 mg. immediately before each dose, in addition
PO: ADULTS, ELDERLY: (Previously tak- to regular monitoring (be alert for fluc-
ing high dose of ACE inhibitor [greater tuations). Assess hydration status. Cor-
than 10 mg enalapril or equivalent] or rect hydration/sodium depletion prior to
ARB [greater than 160 mg valsartan or initiation. Receive medication history and
equivalent]): Initially, 49 mg/51 mg twice screen for interactions, esp. concomitant
daily. (Previously taking low dose of ACE use of aliskiren, ACE inhibitors, ARBs,
inhibitor [10 mg or less of enalapril or potassium-sparing diuretics, potassium
equivalent] or ARB): 24 mg/26 mg twice supplements. Verify negative pregnancy
daily. (Not currently taking an ACE inhibi- status. Question history of hepatic/renal
tor or ARB): 24 mg/26 mg twice daily. impairment, renal artery stenosis; angio-
edema, hypersensitivity reaction.
Dosage in Renal Impairment
Mild to moderate impairment: No INTERVENTION/EVALUATION
dose adjustment. Severe impair- Monitor BMP, esp. serum BUN, creati-
ment: Initially, 24 mg/26 mg twice daily. nine, potassium. Monitor for hyperkale-
Maintenance: May double each dose mia, hypotension. If hypotension occurs,
every 2–4 wks up to 97 mg/103 mg twice place pt in supine position, feet slightly el-
daily based on tolerability. evated; consider interrupting treatment or
altering dose of diuretic, antihypertensive
Dosage in Hepatic Impairment drugs and screen for dehydration/serum
Mild impairment: No dose adjustment. sodium depletion. If pt positive for dehy-
Moderate impairment: Initially, 24 mg/ dration, be cautious with PO/IV adminis-
26 mg twice daily. Maintenance: May tration. Overhydration may exacerbate HF.
double each dose every 2–4 wks up to 97 Assist with ambulation if dizziness occurs.
mg/103 mg twice daily based on tolerabil- Monitor for hypersensitivity reaction,
ity. Severe impairment: Treatment not including angioedema. If angioedema
recommended. occurs, interrupt treatment and institute
therapy to protect airway patency. S
SIDE EFFECTS
Occasional (9%): Cough, dizziness. PATIENT/FAMILY TEACHING
• Go slowly from lying to stand-
ADVERSE EFFECTS/TOXIC ing. • Be cautious of fluid intake. Over-
REACTIONS hydration may lead to worsening of HF,
Angioedema (less than 1% of pts), hypo- while underhydration may lead to low
tension (18% of pts), orthostatic hypoten- blood pressure. • Report urine changes
sion (2% of pts), impairment/decrease such as darkened urine, decreased out-
in renal function due to inhibition of put. • Immediately report allergic reac-
renin-angiotensin-aldosterone system (5% tions such as difficulty breathing, itching,
of pts), elevation of serum creatinine rash, tongue swelling; symptoms of high
greater than 50% from baseline (1.4% of potassium levels such as extreme fatigue,
pts), renal impairment including oliguria, muscle weakness, palpitations; suspected
azotemia, acute renal failure (5% of pts), pregnancy. • Do not breastfeed.
hyperkalemia (12% of pts), serum potas- • Diuretics (water pills) may increase
sium elevation greater than 5.5 mEq/L risk of low pressure or low potassium
(4% of pts) have occurred. levels.

Canadian trade name Non-Crushable Drug High Alert drug


1052 safinamide
increasing dopamine levels and thereby
safinamide increasing dopaminergic activity in the
brain. Therapeutic Effect: Reduces
sa-fin-a-mide effects of Parkinson’s disease.
(Xadago)
Do not confuse safinamide with PHARMACOKINETICS
ethionamide, niacinamide, Absorbed quickly. Widely distributed.
procainamide, pyrazinamide, or Metabolized in liver by nonmicrosomal
Xadogo with Xanax, Xarelto, or enzymatic activity. Protein binding: 88%.
Xalatan. Peak plasma concentration: 2–3 hrs.
Excreted primarily in urine (76%). Half-
uCLASSIFICATION
life: 20–26 hrs.
PHARMACOTHERAPEUTIC: Mono-
amine oxidase type B (MAO-B) inhib- LIFESPAN CONSIDERATIONS
itor. CLINICAL: Antiparkinson agent. Pregnancy/Lactation: Unknown if
distributed in breast milk. Breastfeeding
not recommended. Children: Safety
USES and efficacy not established. Elderly: No
Adjunctive treatment to levodopa/car- age-related precautions noted.
bidopa in pts with Parkinson’s disease
experiencing “off” episodes. Not indi- INTERACTIONS
cated as a monotherapy. DRUG: Amphetamine (or deriva-
tives), cyclobenzaprine, methylphe-
PRECAUTIONS nidate, isoniazid, IV methylene blue
Contraindications: Hypersensitivity to opioids (e.g., fentaNYL, traMADol),
safinamide. Severe hepatic impairment. linezolid, other MAOIs (e.g., phen-
Concomitant use of other MAOIs, potent elzine, selegiline), SNRIs (e.g.,
inhibitors of MAOI (e.g., linezolid), DULoxetine, venlafaxine), tricyclic
amphetamine (and derivatives), cyclo- antidepressants (e.g., amitriptyline)
benzaprine, dextromethorphan, methyl- may increase risk of serotonin syndrome,
phenidate, opioid medications, St. John’s hypertensive crisis; use contraindicated.
wort, selective serotonin-norepinephrine Dextromethorphan may increase
reuptake inhibitors (SNRIs), tricyclic or risk of psychosis, abnormal behavior.
S triazolopyridine antidepressants. Cau- HERBAL: None significant. FOOD: Foods/
tions: Ophthalmic disorders (e.g., any beverages that are high in tyramine
active retinopathy, history of retinal/ (e.g., aged cheese, pickled herring,
macular degeneration, uveitis, inherited red wine) may cause release of norepi-
retinal conditions, history of heredi- nephrine, resulting in hypertension. LAB
tary retina disease, albinism, retinitis, VALUES: May increase serum ALT, AST.
pigmentosa); hypertension, psychiatric
disorders (e.g., schizophrenia, bipolar AVAILABILITY (Rx)
disorder, psychosis); history of dyskine- Tablets: 50 mg, 100 mg.
sia, pts with impulse control disorder;
concomitant use of serotonergic drugs; ADMINISTRATION/HANDLING
moderate hepatic impairment. PO
• Give with or without food at the same
ACTION time every day. • If a dose is missed or
Exact mechanism in Parkinson’s disease vomiting occurs after administration, do
unknown. Selectively inhibits MAO-B not give extra dose. Administer next dose
activity. Inhibits catabolism of dopamine, at regularly scheduled time.

underlined – top prescribed drug


safinamide 1053

INDICATIONS/ROUTES/DOSAGE and cardiac arrhythmia], elevated cre-


Parkinson’s Disease atinine, phosphokinase, myoglobinuria
PO: ADULTS, ELDERLY: 50 mg once daily. [rhabdomyolysis], acute renal failure)
If response is inadequate, may increase to may be associated with rapid dose reduc-
100 mg once daily after 2 wks of treat- tion, withdrawal, changes that increase
ment. (When discontinuing from 100 central dopaminergic tone. Hypersensi-
mg/day, decrease to 50 mg/day for 1 wk tivity reactions (including angioedema),
before discontinuing therapy to avoid risk retinal degeneration, loss of photorecep-
of withdrawal-emergent hyperpyrexia and tors, major psychotic episodes (psycho-
confusion.) sis, hallucinations), dyskinesia, falls were
reported.
Dosage in Renal Impairment
Not specified; use caution. NURSING CONSIDERATIONS
Dosage in Hepatic Impairment BASELINE ASSESSMENT
Mild impairment: No dose adjust- Obtain B/P. Assess symptoms of Parkin-
ment. Moderate impairment: Do son’s disease (e.g., muscular rigidity,
not exceed maximum dose of 50 mg/ pen rolling motion, gait disturbance,
day. Severe impairment: Treatment tremors), emotional state. Receive full
contraindicated. If hepatic impairment medication history and screen for contra-
progresses from moderate to severe indications/interactions. Question history
impairment, permanently discontinue. of ocular disease (personal or family his-
tory), dyskinesia, compulsive/impulsive
SIDE EFFECTS behavior, psychosis, falls. Due to risk of
Frequent (21%): Dyskinesia. Occasional suddenly falling asleep, discuss avoidance
(3%): Nausea. Rare (2% or less): Ortho- of driving vehicles, operating machinery.
static hypotension, anxiety, cough, Conduct baseline ophthalmologic exam,
dyspepsia. visual acuity. Initiate fall precautions.
ADVERSE EFFECTS/TOXIC INTERVENTION/EVALUATION
REACTIONS
Periodically monitor B/P. Assess for clini-
Hypertension, worsening of hyperten- cal improvement, reversal of symptoms
sion, hypertensive crisis was reported. (improvement of hand, head tremor at
Life-threatening serotonin syndrome may rest, mask-like facial expression, mus-
include mental status changes (agitation, S
cular rigidity). Monitor for dyskinesia
hallucinations, delirium, coma), auto- (difficulty with movement), psychosis/hal-
nomic instability (tachycardia, labile blood lucinations; symptoms of serotonin syn-
pressure, dizziness, sweating, flushing, drome, neuroleptic malignant syndrome.
hyperthermia), neuromuscular symptoms Question for episodes of sudden-onset
(tremor, rigidity, myoclonus [localized sleep, accidents, falls, impulsivity. Assess
muscle twitching], hyperactive reflexes, for new-onset ocular/retinal disorders.
incoordination). May cause sudden onset Monitor for hypersensitivity reactions. As-
of sleep (without warning) during normal sist with ambulation.
daily activities or while driving, which may
result in accidents, injury. Impulsive or PATIENT/FAMILY TEACHING
compulsive behaviors including gambling, • Therapy may cause sudden sleep with-
sexual urges, binge eating, intense urge to out drowsiness or warning, which may
spend money have occurred. Neurolep- cause accidents and injury. Avoid tasks that
tic malignant syndrome (hyperpyrexia, require alertness, motor skills until
muscle rigidity, altered mental status, response to drug is established. Driving,
autonomic instability [irregular pulse or operating machinery is extremely
blood pressure, tachycardia, diaphoresis,
Canadian trade name Non-Crushable Drug High Alert drug
1054 salmeterol

risky. • Report symptoms of overproduc- uCLASSIFICATION


tion of serotonin including confusion,
PHARMACOTHERAPEUTIC: Beta 2 -
excessive talking, hallucinations, headache,
adrenergic agonist (long-acting).
hyperactivity, insomnia, racing thoughts,
CLINICAL: Bronchodilator.
seizure activity, tremors; sexual dysfunc-
tion, fever. • Rapid dose reduction or
withdrawal may cause neuroleptic malig- USES
nant syndrome (confusion, high fever, Prevention of exercise-induced bron-
muscle rigidity, high or irregular B/P, heart chospasm, bronchospasm; maintenance
arrhythmias), a life-threatening condi- treatment of asthma and prevention of
tion that can be confused with symptoms of bronchospasm in pts with reversible
severe infection. • Report vision changes; obstructive airway disease, including
impulsive binge eating, gambling, sexual those with symptoms of nocturnal asthma.
urges, inability to stop spending money; Long-term maintenance treatment of
swelling of the face, tongue, throat. • Due bronchospasm associated with COPD
to high risk of drug interactions, do not (including emphysema and chronic
take newly prescribed medication, herbal bronchitis).
supplements unless approved by pre-
scriber who originally started treat- PRECAUTIONS
ment. • Avoid foods high in tyramine Contraindications: Hypersensitivity to sal-
(aged, cured, fermented, pickled, smoked meterol. Treatment of status asthmaticus,
food). acute episodes of asthma or COPD. Use
as monotherapy in treatment of asthma
without concomitant long-term asthma
salmeterol control medication (e.g., inhaled cor-
ticosteroids). Cautions: Not for acute
symptoms; may cause paradoxical bron-
sal-met-er-all chospasm, severe asthma. Cardiovascu-
(Serevent Diskhaler Disk , Ser- lar disorders (coronary insufficiency,
event Diskus) arrhythmias, hypertension), seizure dis-
j BLACK BOX ALERT jLong- orders, diabetes, hyperthyroidism, hepatic
acting beta2-adrenergic agonists
may increase risk of asthma-related impairment, hypokalemia.
S deaths and asthma-related hospital-
izations in pediatric and adolescent ACTION
pts. Use only as adjuvant therapy in Stimulates beta2-adrenergic recep-
pts who are currently receiving but tors in lungs, resulting in relaxation of
not adequately controlled on long-
term asthma control medication. bronchial smooth muscle. Therapeutic
Do not confuse salmeterol with Effect: Relieves bronchospasm, reduc-
Solu-Medrol, or Serevent with ing airway resistance.
Atrovent, Combivent, Serentil, PHARMACOKINETICS
or Sinemet.
Route Onset Peak Duration
FIXED-COMBINATION(S) Inhalation 30–45 2–4 hrs 12 hrs
Advair Diskus: salmeterol/fluticasone (asthma) min
(a corticosteroid): 50 mcg/100 mcg, Inhalation 2 hrs 3.25–4.75 12 hrs
(COPD) hrs
50 mcg/250 mcg, 50 mcg/500 mcg.
Advair HFA: salmeterol/fluticasone Low systemic absorption; acts primarily
(a corticosteroid): 21 mcg/45 mcg, 21 in lungs. Protein binding: 95%. Metabo-
mcg/115 mcg, 21 mcg/230 mcg. lized in liver. Excreted in urine (25%),
feces (60%). Half-life: 5.5 hrs.
underlined – top prescribed drug
salmeterol 1055

LIFESPAN CONSIDERATIONS min before exercise. Additional doses


Pregnancy/Lactation: Unknown if should not be given for 12 hrs. Do not
distributed in breast milk. Children: No administer if already giving salmeterol
age-related precautions in pts older than twice daily.
4 yrs. Elderly: Lower dosages may be Maintenance Therapy for COPD
needed (may be more susceptible to Inhalation: ADULTS, ELDERLY: 1 inhala-
tachycardia, tremors). tion (50 mcg) q12h.
INTERACTIONS Dosage in Renal/Hepatic Impairment
DRUG: Beta blockers (e.g., carvedilol, No dose adjustment.
metoprolol) may reduce effect; may pro-
duce bronchospasm. Strong CYP3A4 SIDE EFFECTS
inhibitors (e.g., clarithromycin, keto- Frequent (28%): Headache. Occasional
conazole, ritonavir), MAOIs (e.g., (7%–3%): Cough, tremor, dizziness, vertigo,
phenelzine, selegiline), tricyclic throat dryness/irritation, pharyngitis. Rare
antidepressants (e.g., amitriptyline, (less than 3%): Palpitations, tachycardia,
doxepin) may increase concentration/ nausea, heartburn, GI distress, diarrhea.
effects (wait 14 days after stopping MAOIs,
tricyclic antidepressants before starting ADVERSE EFFECTS/TOXIC
salmeterol). HERBAL: None significant. REACTIONS
FOOD: None known. LAB VALUES: May May prolong QT interval (can precipitate
decrease serum potassium. May increase ventricular arrhythmias). Hypokalemia,
serum glucose. hyperglycemia may occur.
AVAILABILITY (Rx) NURSING CONSIDERATIONS
Aerosol Powder Breath Activated, Inhala-
BASELINE ASSESSMENT
tion: 50 mcg/inhalation.
Question history of cardiac disease,
ADMINISTRATION/HANDLING hepatic impairment, seizure disorder.
Inhalation Screen for concomitant medications
• Do not shake or prime. Before inhal- known to prolong QT interval. Assess
ing the dose, breath out fully (do not lung sounds, vital signs.
exhale into Diskus device). Activate and INTERVENTION/EVALUATION
use only in level horizontal posi- S
Monitor rate, depth, rhythm, type of res-
tion. • Inhale quickly and deeply
piration; quality/rate of pulse, B/P. Assess
through Diskus. • Hold breath as long
lungs for wheezing, rales, rhonchi. Peri-
as possible before exhaling slowly. • Do
odically evaluate serum potassium levels.
not use a spacer or wash mouthpiece.
PATIENT/FAMILY TEACHING
INDICATIONS/ROUTES/DOSAGE • Not for relief of acute epi-
Maintenance and Prevention Therapy for sodes. • Keep canister at room temper-
Asthma, Bronchospasm ature (cold decreases effects). • Do not
Inhalation: ADULTS, ELDERLY, CHILDREN stop medication or exceed recommended
4 YRS AND OLDER: 1 inhalation (50 mcg) dosage. • Report chest pain, dizzi-
q12h (used in combination with inhaled ness. • Wait at least 1 full min before
corticosteroids not as monotherapy). second inhalation. • Administer dose
30–60 min before exercise when used to
Prevention of Exercise-Induced
prevent exercise-induced broncho-
Bronchospasm
spasm. • Avoid excessive use of caffeine
Inhalation: ADULTS, ELDERLY, CHILDREN 4
derivatives (coffee, tea, colas, chocolate).
YRS AND OLDER: 1 inhalation at least 30
Canadian trade name Non-Crushable Drug High Alert drug
1056 sargramostim
Increases cytoneoplastic cells, activates
sargramostim neutrophils to inhibit tumor cell growth.
sar-gra-moe-stim PHARMACOKINETICS
(Leukine) Route Onset Peak Duration
Do not confuse Leukine with IV (increase 7–14 days N/A 1 wk
leucovorin or Leukeran. WBCs)
uCLASSIFICATION Detected in serum within 5 min after SQ
PHARMACOTHERAPEUTIC: Colony- administration. Peak serum levels:
stimulating factor. CLINICAL: Hemato- 1–3 hrs. Half-life: IV: 1 hr; SQ: 3 hrs.
poietic agent.
LIFESPAN CONSIDERATIONS
USES Pregnancy/Lactation: Unknown if
drug crosses placenta or is distributed
Acute myelogenous leukemia (AML: in breast milk. Children: Safety and effi-
following induction chemother- cacy not established. Elderly: No age-
apy): Shortens time to neutrophil recov- related precautions noted.
ery; reduces incidence of severe infections.
Bone marrow transplant (allogeneic INTERACTIONS
or autologous): For graft failure, engraft- DRUG: May increase adverse effects of
ment delay. Myeloid reconstitution tisagenlecleucel, vaccines (live). May
following allogeneic or autologous bone decrease therapeutic effect of vaccines
marrow transplant. Peripheral stem (live). Corticosteroids (e.g., dexa-
cell transplant (allogeneic or autolo- methasone, predniSONE) may increase
gous): Mobilizes hematopoietic progenitor myeloproliferative effect. HERBAL: None
cells. Hematopoietic radiation injury significant. FOOD: None known. LAB VAL-
syndrome (acute): Treatment to increase UES: May increase serum ALT, AST, bilirubin,
survival due to acute exposure to myelosup- creatinine. May decrease serum albumin.
pressive radiation doses. OFF-LABEL: Pri-
mary prophylaxis of neutropenia. AVAILABILITY (Rx)
PRECAUTIONS Injection, Powder for Reconstitution:
250 mcg.
Contraindications: Hypersensitivity to sar-
S gramostim. Concurrent (24 hrs preceding ADMINISTRATION/HANDLING
or following) myelosuppressive chemo- SQ
therapy or radiation, pts with excessive May be given without further dilution.
leukemic myeloid blasts in bone marrow
or peripheral blood (greater than 10%), IV
known hypersensitivity to yeast-derived
products. Cautions: Preexisting HF, fluid Reconstitution • To 250-mcg vial,
retention, cardiovascular disease, pulmo- add 1 mL Sterile Water for Injection (pre-
nary disease (hypoxia, pulmonary infil- servative free) or Bacteriostatic Water for
trates), renal/hepatic impairment. Injection. Direct diluent to side of vial,
gently swirl contents to avoid foaming; do
ACTION not shake or vigorously agitate. • After
Stimulates proliferation/differentiation and reconstitution, further dilute in 25–50
functional activity of eosinophils, mono- mL 0.9% NaCl to a concentration of 10
cytes, neutrophils, and macrophages. mcg/mL or greater. If final concentration
Therapeutic Effect: Assists bone marrow less than 10 mcg/mL, 1 mg of human
in making new WBCs, increases their che- albumin per 1 mL of 0.9% NaCl should be
motactic, antifungal, antiparasitic activity. added to provide a final albumin

underlined – top prescribed drug


sargramostim 1057
concentration of 0.1% (e.g., 1 mL 5% 500 cells/mm3. Continue until ANC greater
albumin per 50 mL 0.9% NaCl). than 1,500 cells/mm3 for 3 consecutive
days. If WBC greater than 50,000 cells/
b ALERT c Albumin is added before ad-
mm3 and/or ANC greater that 20,000
dition of sargramostim (prevents drug ad- cells/mm3, interrupt treatment or reduce
sorption to components of drug delivery dose by 50%. Discontinue if blast cells
system). appear or underlying disease progresses.
Rate of administration • Give each
single dose over 30 min, 2 hr, 6 hr, or Bone Marrow Transplant Failure,
continuous infusion. Engraftment Delay
Storage • Refrigerate powder, reconsti- IV infusion: ADULTS, ELDERLY: 250 mcg/
tuted solution, diluted solution for injec- m2/day for 14 days. Infuse over 2 hrs. May
tion. • Do not shake. • Reconstituted repeat after 7 days off therapy if engraft-
solutions are clear, colorless. • Use within ment has not occurred. A third course with
6 hrs; discard unused portions. • Use 1 500 mcg/m2/day for 14 days may be tried
dose per vial; do not reenter vial. if engraftment still has not occurred.
IV INCOMPATIBILITIES Stem Cell Transplant, Mobilization
Amphotericin B complex (Abelcet, AmBi- IV, SQ: ADULTS: 250 mcg/m2/day IV (as
some, Amphotec), ondansetron (Zofran). 24-hr infusion) or SQ once daily. Continue
same dose throughout peripheral blood pro-
IV COMPATIBILITIES genitor cell collection. If WBC greater than
Dexamethasone (Decadron), diphen- 50,000 cells/mm3, reduce dose by 50%.
hydrAMINE (Benadryl), famotidine
(Pepcid), granisetron (Kytril), heparin, Stem Cell Transplant, Post-transplant
metoclopramide (Reglan), promethazine IV, SQ: ADULTS, ELDERLY: 250 mcg/m2/
(Phenergan). day IV (as 24-hr infusion) or SQ once
daily beginning immediately following
INDICATIONS/ROUTES/DOSAGE infusion of progenitor cells. Continue until
Neutrophil Recovery Following ANC greater than 1,500 cells/mm3 for 3
Chemotherapy in AML consecutive days.
IV infusion: ADULTS 55 YRS OR OLDER: Hematopoietic Radiation Injury Syndrome
250 mcg/m2/day (as 4-hr infusion) starting (Acute)
approximately 4 days following completion SQ: ADULTS, ELDERLY WEIGHING MORE S
of induction chemotherapy (if day 10 bone THAN 40 KG: 7 mcg/kg once daily. Begin
marrow is hypoplastic with less than 5% treatment as soon as possible after sus-
blasts). Continue until ANC is greater than pected or confirmed exposure to radia-
1,500 cells/mm3 for 3 consecutive days or tion doses greater than 2 (gray) Gy. Do
a maximum of 42 days. If WBC greater than not delay if CBC not available. Continue
50,000 cells/mm3 and/or ANC greater that until ANC remains greater than 1,000/
20,000 cells/mm3, interrupt treatment or cells mm3 for 3 consecutive CBCs (obtain
reduce dose by 50%. q3days) or ANC exceeds 10,000/cells
Myeloid Recovery Following Bone mm3 after radiation-induced nadir.
Marrow Transplant (BMT) Dosage in Renal/Hepatic Impairment
IV infusion: ADULTS, ELDERLY: Usual No dose adjustment.
parenteral dosage: 250 mcg/m2/day (as
2-hr infusion). Begin 2–4 hrs after autolo- SIDE EFFECTS
gous bone marrow infusion and not less Frequent:GI disturbances (nausea, diar-
than 24 hrs after last dose of chemo- rhea, vomiting, stomatitis, anorexia,
therapy or last radiation treatment, when abdominal pain), arthralgia or myal-
post marrow infusion ANC is less than gia, headache, malaise, rash, pruritus.
Canadian trade name Non-Crushable Drug High Alert drug
1058 sarilumab
Occasional: Peripheral edema, weight
gain, dyspnea, asthenia, fever, leukocytosis,
j BLACK BOX ALERT j Tuber-
culosis (TB), invasive fungal infec-
capillary leak syndrome (fluid retention, tions, other opportunistic infections
irritation at local injection site, peripheral leading to hospitalization and death
edema). Rare: Tachycardia, arrhythmias, were reported. Avoid use in pts
thrombophlebitis. with active infection. Withhold
treatment until serious infection is
ADVERSE EFFECTS/ controlled. Test for TB prior to and
during treatment, regardless of ini-
TOXIC REACTIONS tial result; if positive, start treatment
Pleural/pericardial effusion occurs rarely for TB prior to initiation.
after infusion. Do not confuse sarilumab with
adalimumab, avelumab, beli-
NURSING CONSIDERATIONS mumab, brodalumab, dupilum-
BASELINE ASSESSMENT
ab, ipilimumab, nivolumab, or
panitumumab.
Obtain CBC, BMP, LFT, vital signs. Ques-
tion history of cardiac/pulmonary dis- uCLASSIFICATION
ease, renal/hepatic impairment. PHARMACOTHERAPEUTIC: Interleu-
INTERVENTION/EVALUATION kin-6 receptor antagonist. Monoclonal
Monitor CBC with differential, serum re- antibody. CLINICAL: Antirheumatic,
nal/hepatic function, pulmonary function, disease modifying.
vital signs, weight. Monitor for supraven-
tricular arrhythmias during administration USES
(particularly in pts with history of cardiac Treatment of adults with moderately to
arrhythmias). Assess closely for dyspnea severely active rheumatoid arthritis who
during and immediately following infusion have had an inadequate response or intol-
(particularly in pts with history of lung erance to one or more DMARDs. May use
disease). If dyspnea occurs during infu- as monotherapy or in combination with
sion, cut infusion rate by half. If dyspnea nonbiologic DMARDs (do not use in
continues, stop infusion immediately. If combination with biologic DMARDs).
neutrophil count exceeds 20,000 cells/
mm3 or platelet count exceeds 500,000 PRECAUTIONS
cells/mm3, stop infusion or reduce dose Contraindications: Hypersensitivity to
S by half, based on clinical condition of pt. sarilumab. Cautions: Hyperlipidemia,
Blood counts return to normal or baseline hypertriglyceridemia, active hepatic disease
3–7 days after discontinuation of therapy. or hepatic impairment; recent travel or
PATIENT/FAMILY TEACHING residence in endemic TB or mycosis areas;
• Report difficulty breathing, esp. during history of chronic opportunistic infections
or immediately after infusion. • May (esp. bacterial, invasive fungal, mycobac-
increase risk of cardiac arrhythmias; report terial, protozoal, viral, TB); conditions
dizziness, fainting, palpitations. • Treat- predisposing to infection (e.g., diabetes,
ment may cause edema, fluid collection in immunocompromised pts, renal failure,
the lungs or around the heart. open wounds); history of HIV, herpes zoster,
hepatitis B virus (HBV) infection, malignan-
cies; baseline neutropenia, thrombocytope-
nia; pts at risk for GI perforation (Crohn’s
sarilumab disease, diverticulitis, GI tract malignancies,
peptic ulcers, peritoneal malignancies). Not
sar-il-ue-mab recommended in pts with active infection,
(Kevzara) concomitant use of biological DMARDs;

underlined – top prescribed drug


sarilumab 1059
baseline ANC less than 2000 cells/mm3, (approx. 30 min) with needle cap
platelet count less than 150,000 cells/mm3, intact. • Visually inspect for particu-
serum ALT, AST above 1.5 times upper limit late matter or discoloration. Solution
of normal (ULN). should appear clear, colorless to
slightly yellow in color. Do not use if
ACTION solution is cloudy, discolored, or visi-
Binds to interleukin-6 (IL-6) receptor, ble particles are observed.
inhibiting signaling of IL-6, a cytokine Administration • Insert needle sub-
involved in inflammatory and immune cutaneously into upper arms, outer
responses. Therapeutic Effect: Reduces thigh, or abdomen and inject solu-
inflammation of RA. tion. • Do not inject into areas of
active skin disease or injury such as
PHARMACOKINETICS sunburns, skin rashes, inflammation,
Widely distributed. Peak plasma concentra- skin infections, or active psoria-
tion: 2–4 days. Excretion (200 mg dose): sis. • Do not administer IV or intra-
linear, nonsaturable proteolytic pathway. muscularly. • Rotate injection sites.
(150 mg dose): Nonlinear, saturable target Storage • Refrigerate in original car-
medicated pathway. Half-life: Concentra- ton until time of use. • Protect from
tion dependent: 200 mg q2wks (up to 10 light. • May store at room temperature
days); 150 mg q2wks (up to 8 days). for up to 14 days. Once warmed to room
temperature, do not place back into refrig-
LIFESPAN CONSIDERATIONS erator. • Do not freeze or expose to heat-
Pregnancy/Lactation: Crosses the ing sources. • Do not shake.
placental barrier, esp. during the third
trimester. Unknown if distributed in INDICATIONS/ROUTES/DOSAGE
breast milk; however, maternal immu- Note: Do not initiate if ANC is less than
noglobulin G (IgG) is present in breast 2,000 cells/mm3; platelets less than
milk. Children: Safety and efficacy 150,000 cells/mm3; or serum ALT or AST
not established. Elderly: Use caution greater than 1.5 times ULN.
(increased incidence of infections).
Rheumatoid Arthritis
INTERACTIONS SQ: ADULTS, ELDERLY: 200 mg once
DRUG: May decrease therapeutic effect q2wks.
of BCG (intravesical), vaccines (live). S
Dose Modification
May increase adverse effects of belim- Neutropenia
umab, natalizumab, vaccines (live). ANC greater than 1000 cells/
HERBAL: Echinacea may decrease the
mm3: No dose adjustment. ANC 500–
therapeutic effect. FOOD: None known. 1000 cells/mm3: Withhold treatment
LAB VALUES: May increase serum ALT, AST,
until ANC greater than 1000 cells/mm3,
cholesterol, LDL, HDL, triglycerides. May then resume at 150 mg once q2wks.
decrease leukocytes, neutrophils, platelets. May increase to 200 mg once q2wks as
AVAILABILITY (Rx) clinically indicated. ANC less than 500
cells/mm3: Permanently discontinue.
Injection Solution: 150 mg/1.14 mL, 200 Hepatotoxicity
mg/1.14 mL. Serum ALT elevation up to 3 times
ADMINISTRATION/HANDLING ULN: Consider modifying dose of
concomitant DMARDs. Serum ALT
SQ
elevation greater than 3–5 times
Preparation • Remove prefilled ULN: Withhold treatment until serum
syringe from refrigerator and allow ALT less than 3 times ULN, then resume
solution to warm to room temperature at 150 mg once q2wks. May increase to
Canadian trade name Non-Crushable Drug High Alert drug
1060 sarilumab
200 mg once q2wks as clinically indi-
cated. Serum ALT elevation greater NURSING CONSIDERATIONS
than 5 times ULN: Permanently
BASELINE ASSESSMENT
discontinue.
Serious Infection Obtain CBC (note neutrophil, platelet
Withhold treatment until serious infec- count), LFT, lipid panel. Assess onset, lo-
tion is controlled, then resume as clini- cation, duration of pain, inflammation.
cally indicated. Inspect appearance of affected joints for
Thrombocytopenia immobility, deformities. Pts should be
Platelet count 50,000–100,000 cells/ evaluated for active tuberculosis and tested
mm3: Withhold treatment until platelet for latent infection prior to initiation and
count greater than 100,000 cells/mm3, periodically during therapy. Induration of 5
then resume at 150 mg once q2wks. May mm or greater with tuberculin skin testing
increase to 200 mg once q2wks as clini- should be considered a positive test result
cally indicated. Platelet count less than when assessing if treatment for latent tu-
50,000 cells/mm3: Permanently discon- berculosis is necessary. Question history of
tinue if confirmed by repeat testing. chronic infections, opportunistic infections,
herpes infection. Screen for active infection.
Dosage in Renal Impairment Assess skin for open wounds. Question his-
Mild to moderate impairment: No tory of active hepatic disease, GI perfora-
dose adjustment. Severe impair- tion, malignancies, HIV, HBV, hypersensitiv-
ment: Not specified; use caution. ity reactions. Receive full medication history
and screen for interactions. Assess pt’s will-
Dosage in Hepatic Impairment ingness to self-inject medication.
Not specified; use caution.
INTERVENTION/EVALUATION
SIDE EFFECTS
Assess for therapeutic response: relief of
Rare (4%–2%): Injection site reactions pain, stiffness, swelling; increased joint
(pain, erythema, pruritus). mobility; reduced joint tenderness; im-
proved grip strength. Monitor neutrophil
ADVERSE EFFECTS/TOXIC
count, platelet count, LFT 4–6 wks after
REACTIONS
initiation, then q3mos thereafter. Monitor
Serious, sometimes fatal, infections includ- lipid panel 4–6 wks after initiation, then
ing aspergillosis, candidiasis, cellulitis, q6mos thereafter. Monitor for symptoms
S Cryptococcus, histoplasmosis, pneumo- of tuberculosis, including those who tested
nia, sepsis, tuberculosis; bacterial, myco- negative for latent tuberculosis infection
bacterial, invasive fungal, opportunistic, prior to initiating therapy. Interrupt or dis-
viral infections were reported. Nasophar- continue treatment if serious infection, op-
yngitis, upper respiratory tract infections, portunistic infection, or sepsis occurs and
urinary tract infections occurred in 2–4% initiate appropriate antimicrobial therapy.
of pts. Neutropenia may increase risk of Closely monitor for HBV reactivation.
serious infection. GI perforation may
occur, esp. in pts with history of diver- PATIENT/FAMILY TEACHING
ticulitis or concomitant use of NSAIDs, • Treatment may depress your immune
corticosteroids. May increase risk for new system and reduce your ability to fight
malignancies. Hypersensitivity reactions infection. Report symptoms of infection
including rash, urticaria reported in less such as body aches, burning with urination,
than 1% of pts. May increase risk of HBV chills, cough, fatigue, fever. Avoid those with
reactivation, which may result in fulminant active infection. • Do not receive live vac-
hepatitis, hepatic failure, death. Immuno- cines. • Expect frequent tuberculosis
genicity (auto-sarilumab antibodies) was screening. Report travel plans to possible
reported.
underlined – top prescribed drug
sAXagliptin 1061

endemic areas. • A health care provider use of strong CYP3A4 inhibitors (e.g.,
will show you how to properly prepare and clarithromycin).
inject medication. You must demonstrate ACTION
correct preparation and injection tech-
niques before using medication at Slows the inactivation of incretin hormones
home. • Report allergic reactions such as by inhibiting DDP-4 enzyme. Incretin hor-
itching, hives, rash. • Immediately report mones increase insulin synthesis/release
severe or persistent abdominal pain, bloody from pancreas and decrease glucagon
stool, fever; may indicate tear in GI secretion. Therapeutic Effect: Regulates
tract. • Treatment may cause reactivation glucose homeostasis.
of HBV, new cancers. • Therapy may PHARMACOKINETICS
decrease platelet count, which may increase
risk of bleeding. • Report liver problems Route Onset Peak Duration
such as bruising, confusion, amber or Oral — — 24 hrs
dark-colored urine; right upper abdominal Rapidly absorbed following PO adminis-
pain; yellowing of the skin or eyes. tration. Extensively metabolized. Excreted
by both renal and hepatic pathways.
Half-life: 2.5 hrs; metabolite, 3.1 hrs.
sAXagliptin
LIFESPAN CONSIDERATIONS
sax-a-glip-tin Pregnancy/Lactation: Unknown if dis-
(Onglyza) tributed in breast milk. Children: Safety
Do not confuse SAXagliptin with and efficacy not established. Elderly: Age-
SITagliptin or SUMAtriptan. related renal impairment may require dos-
age adjustment.
FIXED-COMBINATION(S)
Kombiglyze XR: SAXagliptin/met- INTERACTIONS
FORMIN (an antidiabetic): 2.5 mg/ DRUG: May increase hypoglycemic effects
1,000 mg, 5 mg/500 mg, 5 mg/1,000 of insulin, sulfonylureas (e.g., glipi-
mg. ZIDE, glyBURIDE). Strong CYP3A4
inhibitors (e.g., clarithromycin, keto-
uCLASSIFICATION conazole) may increase concentration/
PHARMACOTHERAPEUTIC: DDP-4 effect. CYP3A4 inducers (e.g., carBA- S
inhibitor (gliptins). CLINICAL: Antidia- Mazepine, phenytoin, rifAMPin) may
betic agent. decrease concentration/effect. HERBAL:
Herbals with hypoglycemic proper-
USES ties (e.g., fenugreek) may increase
effect. FOOD: Grapefruit products
Adjunctive treatment to diet and exercise
may increase concentration. LAB VAL-
to improve glycemic control in pts with
UES: May slightly decrease WBCs, lym-
type 2 diabetes as monotherapy or in com-
phocytes. May increase serum creatinine.
bination with other antidiabetic agents.
AVAILABILITY (Rx)
PRECAUTIONS
Contraindications: Hypersensitivity to Tablets, Film-Coated: 2.5 mg, 5 mg.
SAXagliptin. Type 1 diabetes, ketoacido-
ADMINISTRATION/HANDLING
sis. Cautions: Concurrent use of other
glucose-lowering agents may increase PO
risk of hypoglycemia, moderate to severe • May give without regard to food. • Do
renal impairment, end-stage renal dis- not break, crush, dissolve, or divide film-
ease requiring hemodialysis, concurrent coated tablets.
Canadian trade name Non-Crushable Drug High Alert drug
1062 scopolamine

INDICATIONS/ROUTES/DOSAGE PATIENT/FAMILY TEACHING


Type 2 Diabetes • Diabetes requires lifelong control.
PO: ADULTS, ELDERLY: 2.5 or 5 mg once Prescribed diet and exercise are principal
daily. Concurrent strong CYP3A4 parts of treatment; do not skip or delay
inhibitors (e.g., ketoconazole): 2.5 meals. • Continue to adhere to dietary
mg once daily. Hemodialysis: Give dose instructions, regular exercise program,
after dialysis. regular testing of blood glucose. • When
taking combination drug therapy or when
Dosage in Renal Impairment
glucose demands are altered (fever,
Mild impairment: No dose adjustment.
infection, trauma, stress, heavy physical
Moderate to severe impairment: CrCl
activity), have a source of glucose avail-
less than 50 mL/min: 2.5 mg once daily. able to treat symptoms of hypoglycemia.
Dosage in Hepatic Impairment
No dose adjustment.
SIDE EFFECTS scopolamine
Occasional (7%): Headache. Rare
(3%–1%): Peripheral edema, sinusitis, skoe-pol-a-meen
abdominal pain, gastroenteritis, vomit- (Trans-Derm Scop, Buscopan )
ing, rash. FIXED-COMBINATION(S)
ADVERSE EFFECTS/ Donnatal: scopolamine/atropine
TOXIC REACTIONS (anticholinergic)/hyoscyamine (anti­
Lymphopenia, rash occur rarely. Upper cholinergic)/PHENobarbital (sedative):
respiratory tract infection, urinary tract 0.0065 mg/0.0194 mg/0.1037 mg/
infection occur in approximately 7% of pts. 16.2 mg.
uCLASSIFICATION
NURSING CONSIDERATIONS
PHARMACOTHERAPEUTIC: Anticho-
BASELINE ASSESSMENT linergic. CLINICAL: Antinausea,
Check serum blood glucose before antie­metic.
administration. Discuss lifestyle to de-
termine extent of learning, emotional
S needs. Ensure follow-up instruction if pt USES
or family does not thoroughly understand Prevention of motion sickness, postop nau-
diabetes management or glucose-testing sea/vomiting. OFF-LABEL: Breakthrough
technique. treatment of nausea/vomiting associated
with chemotherapy.
INTERVENTION/EVALUATION
Assess for hypoglycemia (diaphoresis, PRECAUTIONS
tremors, dizziness, anxiety, headache, Contraindications: Hypersensitivity to sco-
tachycardia, perioral numbness, hun- polamine. Narrow-angle glaucoma. Cau-
ger, diplopia, difficulty concentrating), tions: Hepatic/renal impairment, cardiac
hyperglycemia (polyuria, polyphagia, disease (hypertension, HF), seizure dis-
polydipsia, nausea, vomiting, dim vision, order, psychoses, coronary artery disease,
fatigue, deep, rapid breathing). Be alert prostatic hyperplasia, urinary retention,
to conditions that alter glucose require- reflux esophagitis, ulcerative colitis, hyper-
ments (fever, increased activity or stress, thyroidism, GI obstruction, hiatal hernia,
surgical procedures). elderly pts.

underlined – top prescribed drug


secukinumab 1063

ACTION (5%–1%): Dizziness, restlessness, hallu-


Competitively inhibits action of acetylcho- cinations, confusion, difficulty urinating,
line in smooth muscle, secretory glands, rash.
and CNS.  Therapeutic Effect: Prevents
ADVERSE EFFECTS/
motion-induced nausea/vomiting.
TOXIC REACTIONS
LIFESPAN CONSIDERATIONS None known.
Pregnancy/Lactation: Crosses pla-
NURSING CONSIDERATIONS
centa; unknown if distributed in breast
milk. Children: May be more suscep- BASELINE ASSESSMENT
tible to adverse effects. Elderly: Diz- Assess for use of other CNS depressants,
ziness, hallucinations, confusion may drugs with anticholinergic action, his-
require dosage adjustment. Use caution. tory of narrow-angle glaucoma. Question
medical history as listed in Precautions.
INTERACTIONS
Transdermal: DRUG: None sig- INTERVENTION/EVALUATION
nificant. HERBAL: None significant. Monitor for dehydration. Observe for im-
FOOD: Grapefruit products may provement of symptoms.
increase concentration/effects. LAB VAL-
PATIENT/FAMILY TEACHING
UES: May interfere with gastric secretion
test. • Avoid tasks requiring alertness, motor
skills until response to drug is established
AVAILABILITY (Rx) (may cause drowsiness, disorientation,
Transdermal System: (Trans-Derm Scop): confusion). • Use only 1 patch at a
1.5 mg. time; do not cut. • Wash hands after
administration.
ADMINISTRATION/HANDLING
Transdermal
• Apply patch to hairless area behind
one ear. • If dislodged or on for more secukinumab
than 72 hrs, replace with fresh
patch. • Do not cut/trim. • Limit sek-ue-kin-ue-mab
contact with water. (Cosentyx, Cosentyx Sensor Pen)
Do not confuse secukinumab S
INDICATIONS/ROUTES/DOSAGE with canakinumab, ranibizum-
Prevention of Motion Sickness ab, trastuzumab, ustekinumab
Transdermal: ADULTS: One system at
uCLASSIFICATION
least 4 hrs prior to exposure and q72h
as needed. PHARMACOTHERAPEUTIC: Mono-
clonal antibody. Human interleukin-
Postop Nausea/Vomiting 17A antagonist. CLINICAL: Antipso-
Transdermal: ADULTS, ELDERLY: 1 sys- riasis agent.
tem no sooner than 1 hr before surgery
and removed 24 hrs after surgery.
USES
Dosage in Renal/Hepatic Impairment Treatment of moderate to severe plaque
No dose adjustment. psoriasis in adult pts who are candidates
for systemic therapy or phototherapy, active
SIDE EFFECTS psoriatic arthritis (PsA), active ankylosing
Frequent (greater than 15%): Dry mouth, spondylitis (AS).
drowsiness, blurred vision. Rare

Canadian trade name Non-Crushable Drug High Alert drug


1064 secukinumab

PRECAUTIONS ADMINISTRATION/HANDLING
Contraindications: Hypersensitivity to SQ
secukinumab. Cautions: Elderly, active • Follow instructions for preparation
Crohn’s disease, HIV infection, con- according to manufacturer guidelines.
comitant use of immunosuppressants; Administration • Insert needle sub-
conditions predisposing to infections cutaneously into upper arms, outer thigh,
(e.g., diabetes, renal failure, immuno- or abdomen and inject solution. • Do
compromised pts, open wounds); hyper- not inject into areas of active skin disease
sensitivity to latex (injector pen/prefilled or injury such as sunburns, skin rashes,
syringe), preexisting or recent-onset CNS inflammation, skin infections, or active
demyelinating disorders (e.g., multiple psoriasis. • Rotate injection sites.
sclerosis, polyneuropathy); exposure to Storage • Refrigerate until time of
tuberculosis. Administration of live vac- use. • Allow injector pen/prefilled
cines not recommended. syringe/vial to warm to room temperature
before use (15–30 min). Do not freeze.
ACTION
Selectively binds to the interleukin- INDICATIONS/ROUTES/DOSAGE
17A (IL-17A) cytokine, inhibiting its Plaque Psoriasis
interaction with the IL-17 receptor. SQ: ADULTS, ELDERLY: 300 mg every wk
IL-17A is involved in inflammatory for 5 doses, then 300 mg q4wks. (Some
and immune responses. Therapeutic pts may only require 150 mg.)
Effect: Inhibits release of proinflam-
matory cytokines. PsA, AS
Note: With coexistent plaque psoriasis,
PHARMACOKINETICS use dose for plaque psoriasis.
Widely distributed. Degraded into small SQ: ADULTS, ELDERLY: Initially, 150 mg at
peptides and amino acids via catabolic wks 0, 1, 2, 3, and 4, then q4wks or 150
pathway. Peak plasma concentration: mg q4wks. For active PsA, may consider
6 days. Steady state reached in 24 wks. dose of 300 mg.
Excretion not defined. Half-life: 22–31
days. Dosage in Renal/Hepatic Impairment
Not studied; use caution.
LIFESPAN CONSIDERATIONS
S SIDE EFFECTS
Pregnancy/Lactation: Unknown if dis-
tributed in breast milk. Children: Safety Rare (4%–1%): Diarrhea, urticaria, rhi­-
and efficacy not established. Elderly: No norrhea.
age-related precautions noted. ADVERSE EFFECTS/
INTERACTIONS TOXIC REACTIONS
DRUG: May decrease efficacy/immune May increase risk of infection including
response of live vaccines; may increase tuberculosis. Infection processes including
risk of toxic effects of live vaccines. nasopharyngitis (11% of pts), upper respi-
HERBAL: Echinacea may decrease the ratory tract infection (2.5% of pts), muco-
therapeutic effect. FOOD: None known. cutaneous infection with candida (1.2% of
LAB VALUES: None significant. pts), rhinitis, pharyngitis, oral herpes (1% of
pts) have occurred. May cause exacerbation
AVAILABILITY (Rx) of Crohn’s disease. Hypersensitivity reac-
Injector Pen: 150 mg/mL solution. Pre- tions including anaphylaxis were reported.
filled Syringe: 150 mg/mL solution. Immunogenicity (auto-secukinumab anti-
bodies) occurred in less than 1% of pts.

underlined – top prescribed drug


selegiline 1065

NURSING CONSIDERATIONS selegiline


BASELINE ASSESSMENT
se-le-ji-leen
Obtain baseline vital signs. Pts should (Emsam, Zelapar)
be evaluated for active tuberculosis and
tested for latent infection prior to initi- j BLACK BOX ALERT jAntide-
pressants increase risk of suicidal
ating treatment and periodically during thoughts and behavior in pediatrics
therapy. Induration of 5 mm or greater and young adults. Monitor closely
with tuberculin skin testing should be for changes in behavior, suicidal
considered a positive test result when ideation.
assessing if treatment for latent tuber- Do not confuse Eldepryl with
culosis is necessary. Antifungal therapy Elavil or enalapril, selegiline
should be considered for those who with Salagen, sertraline, or
reside or travel to regions where myco- Stelazine, or Zelapar with Zale-
ses are endemic. Do not initiate therapy plon, Zemplar, or ZyPREXA.
during active infection. Question history uCLASSIFICATION
of active Crohn’s disease, hepatitis B or C
virus infection, HIV infection, demyelin- PHARMACOTHERAPEUTIC: MAOI.
ating disorders, cardiovascular disease; CLINICAL: Antiparkinson agent, anti­
concomitant use of immunosuppressive depressant.
agents.
INTERVENTION/EVALUATION USES
Monitor skin for disease improvement. Oral: Adjunct to levodopa/carbidopa in
Monitor for symptoms of tuberculosis, treatment of Parkinson’s disease. Trans-
including those who tested negative dermal: Treatment of major depressive
for latent tuberculosis infection prior disorder (MDD). OFF-LABEL: Treatment
to initiating therapy. Interrupt or dis- of ADHD, early Parkinson’s disease.
continue treatment if serious infec-
tion, opportunistic infection, or sepsis PRECAUTIONS
occurs. Monitor for hypersensitivity Contraindications: Hypersensitivity to
reaction. selegiline. Concurrent use of meperidine.
Orally Disintegrating Tablet (addi-
PATIENT/FAMILY TEACHING tional): Concurrent use of cyclobenza- S
• Treatment may depress your immune prine, dextromethorphan, methadone,
system response and reduce your ability St. John’s wort, traMADol, oral selegiline,
to fight infection. Report symptoms of other MAOIs within 14 days of selegiline.
infection such as body aches, chills, Transdermal (additional): Pheo-
cough, fatigue, fever. Avoid those with chromocytoma; concurrent use of
active infection. • Do not receive live buPROPion, SSRIs (e.g., FLUoxetine),
vaccines. • Expect frequent tuberculo- SNRIs (e.g., DULoxetine), tricyclic anti-
sis screening. • Report travel plans to depressants, busPIRone, traMADol,
possible endemic areas. • Injector methadone, dextromethorphan, St. John’s
pen/prefilled syringe should not be used wort, mirtazapine, cyclobenzaprine, oral
by pts with latex allergy. • Immediately selegiline, other MAOIs, carBAMazepine,
report itching, hive, rash, swelling of the OXcarbazepine, sympathomimetics (e.g.,
face or tongue; may indicate allergic amphetamines, cold products containing
reaction. • Treatment may cause wors- vasoconstrictors). Elective surgery requir-
ening of Crohn’s disease. ing general anesthesia, local anesthesia
containing sympathomimetics; foods high

Canadian trade name Non-Crushable Drug High Alert drug


1066 selegiline
in tyramine content. Cautions: Renal/ adverse effects. HERBAL: Herbals with
hepatic impairment, depression, elderly hypotensive properties (e.g., garlic,
pts, major psychiatric disorder; pts at high ginger, ginkgo biloba) may increase
risk of suicide; pts at high risk of hypoten- hypotensive effect. FOOD: Tyramine-
sion (cerebrovascular disease, cardiovas- rich foods may produce hypertensive
cular disease, hypovolemia). reactions. LAB VALUES: None significant.
ACTION AVAILABILITY (Rx)
Irreversibly inhibits activity of mono- Capsules: 5 mg. Tablets: 5 mg. Tablets,
amine oxidase type B (enzyme that breaks Orally Disintegrating: (Zelapar): 1.25 mg.
down DOPamine), thereby increas- Transdermal: (Emsam): 6 mg/24 hrs, 9
ing dopaminergic action. Therapeu- mg/24 hrs, 12 mg/24 hrs.
tic Effect: Relieves signs/symptoms of
Parkinson’s disease (tremor, akinesia, ADMINISTRATION/HANDLING
posture/equilibrium disorders, rigid- PO
ity). Improves mood with MDD. • Give without regard to food. • Avoid
tyramine-containing foods, large quanti-
PHARMACOKINETICS ties of caffeine-containing beverages.
Route Onset Peak Duration
PO (Orally Disintegrating Tablets)
PO 1 hr — 24–72
hrs • Give in morning before breakfast and
without liquid. • Peel off backing with
Rapidly absorbed from GI tract. Crosses dry hands (do not push tablets through
blood-brain barrier. Protein binding: foil). • Immediately place on top of
90%. Metabolized in liver. Primarily tongue, allow to disintegrate. • Avoid
excreted in urine. Half-life: PO: 10 food, liquids for 5 min before and after
hrs. Transdermal: 18–25 hrs. taking selegiline.
LIFESPAN CONSIDERATIONS Transdermal
Pregnancy/Lactation: Unknown if • Apply to dry, intact skin on upper
drug crosses placenta or is distributed torso or thigh, outer surface of upper
in breast milk. Children: Safety and effi- arm. • Avoid exposure to external heat
cacy not established. Elderly: No age- source. • Normal exposure to water
S related precautions noted. unlikely to affect adhesion. • If patch
becomes loose, press back into place. If
INTERACTIONS patch falls off again, apply a new patch;
DRUG: FLUoxetine, fluvoxaMINE, follow same dose schedule. • Rotate
PARoxetine, sertraline, venlafaxine application sites.
may cause mania, serotonin syndrome
(altered mental status, restlessness, dia- INDICATIONS/ROUTES/DOSAGE
phoresis, diarrhea, fever). Meperidine Adjunctive Treatment of Parkinson’s
may cause serotonin syndrome reaction Disease
(e.g., excitation, diaphoresis, rigidity, PO: ADULTS: (Capsule, Tablet): 5 mg
hypertension/hypotension, coma, death). at breakfast and lunch, given concomi-
Tricyclic antidepressants (e.g., tantly with each dose of carbidopa and
amitriptyline, doxepin) may cause levodopa. ELDERLY: Initially, 5 mg in the
diaphoresis, hypertension, syncope, morning. May increase up to 10 mg/day.
altered mental status, hyperpyrexia, sei- ADULTS, ELDERLY: (Orally Disintegrat-
zures, tremors (wait 14 days between ing Tablet): Initially, 1.25 mg daily for
stopping selegiline and starting tricyclic at least 6 wks. May increase to maximum
antidepressants). Alcohol may increase of 2.5 mg/day.

underlined – top prescribed drug


semaglutide 1067
Major Depressive Disorder
rigidity). Monitor for unusual behavior,
Transdermal: ADULTS: Initially, 6 mg/
worsening depression, suicidal ideation,
24 hrs. May increase in 3 mg/24 hrs
especially at initiation of therapy or with
increments at minimum of 2 wks. Maxi-
changes in dosage.
mum: 12 mg/24 hrs. ELDERLY: Maxi-
mum: 6 mg/24 hrs. PATIENT/FAMILY TEACHING
• Tolerance to dizziness, light-headed-
Dosage in Renal/Hepatic Impairment
ness develops during therapy. • To
Orally disintegrating tablet: Not
reduce hypotensive effect, slowly go from
recommended in severe impairment.
lying to standing. • Avoid tasks that
Oral: Use caution. Transdermal: No
require alertness, motor skills until
dose adjustment.
response to drug is established. • Dry
SIDE EFFECTS mouth, drowsiness, dizziness may be an
expected response to drug. • Avoid alco-
Frequent (10%–4%): Nausea, dizziness,
hol. • Report worsening depression,
light-headedness, syncope, abdominal
unusual behavior, thoughts of sui-
discomfort. Occasional (3%–2%): Con-
cide. • Avoid tyramine-rich foods. • Do
fusion, hallucinations, dry mouth, vivid
not take newly prescribed medications
dreams, dyskinesia. Rare (1%): Headache,
unless approved by prescriber who origi-
myalgia, anxiety, diarrhea, insomnia.
nally started treatment. • Do not take
ADVERSE EFFECTS/ herbal supplements.
TOXIC REACTIONS
Symptoms of overdose may vary from
CNS depression (sedation, apnea, cardio- semaglutide
vascular collapse, death) to severe para-
doxical reactions (hallucinations, tremor, sem-a-gloo-tide
seizures). Impaired motor coordination, (Ozempic, Rybelsus)
(loss of balance, blepharospasm, facial j BLACK BOX ALERT jThyroid
grimaces, feeling of heaviness in lower C-cell tumors have occurred in
extremities), depression, nightmares, delu- rodent studies with glucagon-
sions, overstimulation, sleep disturbance, like peptide-1 (GLP-1) receptor
anger, hallucinations, confusion may occur. agonists; unknown if relevant in
humans. Contraindicated in pts with
a personal/family history of medul- S
NURSING CONSIDERATIONS lary thyroid carcinoma or in pts
BASELINE ASSESSMENT
with multiple endocrine neoplasia
syndrome type 2.
Receive full medication history and Do not confuse semaglutide
screen for contraindications/interactions. with albiglutide, dulaglutide,
Question medical history as listed in Pre- liraglutide, or teduglutide.
cautions. Assess current state of mental
health. uCLASSIFICATION

INTERVENTION/EVALUATION PHARMACOTHERAPEUTIC: Glucagon-


like peptide-1 (GLP-1) receptor ago-
Be alert to neurologic effects (headache, nist. CLINICAL: Antidiabetic.
lethargy, mental confusion, agitation).
Monitor for evidence of dyskinesia (diffi-
culty with movement). Assess for clinical USES
reversal of symptoms (improvement of Adjunct to diet and exercise to improve
tremors of head/hands at rest, mask-like glycemic control in adults with type 2 dia-
facial expression, shuffling gait, muscular betes mellitus.

Canadian trade name Non-Crushable Drug High Alert drug


1068 semaglutide

PRECAUTIONS AVAILABILITY (Rx)


Contraindications: Hypersensitivity to Injection Solution, Prefilled Injector
semaglutide. Personal/family history of Pen: 1 mg/dose or 0.25 mg or 0.5 mg
medullary thyroid carcinoma (MTC). Pts per dose (2 mg/1.5 mL). Tablets: 3 mg,
with multiple endocrine neoplasia syn- 7 mg, 14 mg.
drome type 2 (MEN2). Cautions: Mild
to moderate gastroparesis, renal impair- ADMINISTRATION/HANDLING
ment. History of pancreatitis. Not recom- PO
mended in pts with severe GI disease, • Administer on an empty stomach, at
diabetic ketoacidosis, type 1 diabetes least 30 min before the first food intake,
mellitus, or pancreatitis, or for use as beverage, or other oral medications of the
first-line treatment regimen. day. • Take with 4 oz of plain water only.
Eat 30–60 min after dose. • Administer
ACTION whole; do not break, cut, or crush. Tablets
Agonist of human glucagon-like pep- cannot be chewed.
tide-1 (GLP-1). Increases glucose-
dependent insulin secretion. Decreases SQ
inappropriate glucagon secretion. Guidelines • Administer any time of the
Slows gastric emptying. Therapeutic day, without regard to food, on the same
Effect: Augments glucose-dependent day of each wk. May change administration
insulin secretion. day if the time between two doses is at least
2 days. • If dose is missed, administer
PHARMACOKINETICS within 5 days of missed dose. If more than 5
Widely distributed. Metabolized by pro- days pass after missed dose, wait until next
teolytic enzymes via protein degradation regularly scheduled dose.
into small peptides, amino acids. Protein Preparation • Visually inspect for par-
binding: greater than 99%. Peak plasma ticulate matter or discoloration. Solution
concentration: 1–3 days. Steady state should appear clear, colorless, and free of
reached in 4–5 wks. Excreted in urine particles. Do not use if solution is cloudy,
(3% unchanged), feces. Half-life: 7 discolored, or visible particles are observed.
days. Administration • Insert needle
subcutaneously into abdomen, outer
LIFESPAN CONSIDERATIONS thigh, or upper arm, and inject solu-
S Pregnancy/Lactation: Unknown if dis- tion. • Do not inject into areas of
tributed in breast milk. Due to extended active skin disease or injury such as sun-
clearance period, recommend discon- burns, skin rashes, inflammation, skin
tinuation of therapy at least 2 mos before infections, or active psoriasis. • Do
planned pregnancy. Children: Safety not administer IV or intramuscu-
and efficacy not established. Elderly: No lar. • Rotate injection sites.
age-related precautions noted. Storage • Refrigerate unused injector
pens. • Once used, may refrigerate or store
INTERACTIONS at room temperature for up to 56 days. • Do
DRUG: May increase hypoglycemic effect not freeze. • Protect from sunlight.
of insulins, sulfonylureas (e.g.,
glipiZIDE, glyBURIDE). HERBAL: INDICATIONS/ROUTES/DOSAGE
Herbals with hypoglycemic proper- Type 2 Diabetes Mellitus
ties (e.g., fenugreek) may increase SQ: ADULTS, ELDERLY: Initially, 0.25 mg
effect. FOOD: None known. LAB VAL- once wkly for 4 wks, then increase to 0.5
UES: Expected to decrease serum glu- mg once wkly for at least 4 wks. If glyce-
cose, Hgb A1c. May increase serum mic response is inadequate, may further
amylase, lipase. increase to a maximum of 1 mg once wkly.
underlined – top prescribed drug
semaglutide 1069
PO: ADULTS, ELDERLY: Initially, 3 mg once INTERVENTION/EVALUATION
daily for 30 days, then increase to 7 mg
Monitor capillary blood glucose levels, Hgb
once daily for at least 30 days. May fur-
A1c; renal function in pts with renal impair-
ther increase to 14 mg once daily. Note:
ment reporting severe GI symptoms such
The 3 mg dose is intended only for ther-
as diarrhea, gastroparesis, vomiting. Moni-
apy initiation.
tor for hypersensitivity reaction. Screen
Dosage in Renal/Hepatic Impairment for thyroid tumors (dysphagia, dyspnea,
Mild to severe impairment: No dose persistent hoarseness, neck mass). If tu-
adjustment. mor is suspected, consider endocrinologist
consultation. Clinical significance of serum
SIDE EFFECTS calcitonin level or thyroid ultrasound with
Occasional (15%–5%): Nausea, vomiting, GLP-1–associated thyroid tumors is de-
diarrhea, abdominal pain, constipation. bated/unknown. Assess for hypoglycemia
Rare (less than 1%): Injection site reac- (anxiety, confusion, diaphoresis, diplo-
tions (pain, erythema), fatigue, dysgeu- pia, dizziness, headache, hunger, perioral
sia, dizziness. numbness, tachycardia, tremors), hyper-
glycemia (confusion, fatigue, Kussmaul
ADVERSE EFFECTS/TOXIC breathing, nausea, polyuria, vomiting).
REACTIONS Screen for glucose-altering conditions:
May increase risk of acute renal failure or fever, stress, surgical procedures, trauma.
worsening of chronic renal impairment Monitor for pancreatitis (severe, steady
(esp. with dehydration), severe gastropa- abdominal pain often radiating to the back
resis, pancreatitis, thyroid C-cell tumors. [with or without vomiting]). Encourage
Hypersensitivity reactions including ana- fluid intake. Monitor I&Os.
phylaxis, angioedema were reported. May PATIENT/FAMILY TEACHING
increase risk of hypoglycemia when used
with other hypoglycemic agents, insulin. Dia- • A health care provider will show you how
betic retinopathy complications reported in to properly prepare and inject medication.
1% of pts. Worsening of diabetic retinopathy You must demonstrate correct preparation
has been associated with rapid improvement and injection techniques before using medi-
of glucose control. Cholelithiasis reported in cation at home. • Diabetes mellitus
2% of pts. Immunogenicity (anti-semaglutide requires lifelong control. Diet and exer-
antibody formation) reported in 1% of pts. cise are principal parts of treatment; do not
skip or delay meals. • Test blood sugar S
NURSING CONSIDERATIONS regularly. • Monitor daily calorie intake.
• When taking additional medications to
BASELINE ASSESSMENT lower blood sugar or when glucose demands
Obtain baseline fasting glucose level, are altered (fever, infection, stress, trauma),
Hgb A1c. Obtain BUN, serum creatinine, have low blood sugar treatment available
eGFR, CrCl in pts with renal impairment. (glucagon, oral dextrose). • Therapy may
Question history of medullary thyroid increase risk of thyroid cancer; report lumps
carcinoma, multiple endocrine neoplasia or swelling of the neck, hoarseness, short-
syndrome type 2, hypersensitivity reac- ness of breath, trouble swallowing. • Per-
tion, pancreatitis. Screen for use of other sistent, severe abdominal pain that radiates
hypoglycemic agents, insulin. Assess pt’s to the back (with or without vomiting) may
understanding of diabetes management, indicate acute pancreatitis. • Report aller-
routine home glucose monitoring. Assess gic reactions of any kind, esp. difficulty
hydration status. Obtain dietary consult breathing, itching, rash, swelling of the face
for nutritional education. Assess pt’s will- or throat. • Kidney injury or kidney failure
ingness to self-inject medication. may occur; report decreased urine output,
amber-colored urine, flank pain.
Canadian trade name Non-Crushable Drug High Alert drug
1070 sertraline
synaptic receptor sites. Thera-
post­
sertraline peutic Effect: Relieves depression,
reduces obsessive-compulsive behavior,
ser-tra-leen decreases anxiety.
(Zoloft)
j BLACK BOX ALERT j Increased PHARMACOKINETICS
risk of suicidal ideation and behavior Incompletely, slowly absorbed from GI
in children, adolescents, young adults
18–24 yrs with major depressive tract; food increases absorption. Protein
disorder, other psychiatric disorders. binding: 98%. Widely distributed. Metab-
Do not confuse sertraline with olized in liver. Excreted in urine (45%),
selegiline, Serentil, or Serevent, feces (45%). Not removed by hemodialy-
or Zoloft with Zocor. sis. Half-life: 26 hrs.

uCLASSIFICATION LIFESPAN CONSIDERATIONS


PHARMACOTHERAPEUTIC: Selective Pregnancy/Lactation: Unknown if
serotonin reuptake inhibitor. CLINI- drug crosses placenta or is distributed
CAL: Antidepressant, anxiolytic, ob- in breast milk. Children: Children and
sessive-compulsive disorder adjunct. adolescents are at increased risk for sui-
cidal ideation and behavior or worsening
of depression, esp. during the first few
USES mos of therapy. Elderly: No age-related
Treatment of major depressive disorders, precautions noted, but lower initial dos-
panic disorder, obsessive-compulsive dis- ages recommended.
order (OCD), post-traumatic stress dis-
order (PTSD), premenstrual dysphoric INTERACTIONS
disorder (PMDD), social anxiety disorder. DRUG: Alcohol, disulfiram may increase
OFF-LABEL: Eating disorders, bulimia ner- adverse effects. Anticoagulants (e.g.,
vosa, generalized anxiety disorder (GAD). heparin, rivaroxaban, warfarin),
antiplatelets (e.g., aspirin, clopi-
PRECAUTIONS dogrel), NSAIDs (e.g., ibuprofen,
Contraindications: Hypersensitivity to ketorolac, naproxen) may increase
sertraline. MAOI use within 14 days (con- risk of bleeding. MAOIs (e.g., phen-
currently or within 14 days of stopping an elzine, selegiline) may cause neuro-
S MAOI or sertraline). Concurrent use of leptic malignant syndrome, serotonin
oral concentrate (contains alcohol) with syndrome. Concomitant use of other
disulfiram. Concurrent use with pimo- serotonergic drugs (e.g., busPIRone,
zide; initiation in pts treated with linezolid carBAMazepine, fentaNYL, linezolid,
or methylene blue. Cautions: Seizure dis- lithium, SNRIs [e.g., DULoxetine,
order, hepatic impairment, pts at risk for venlafaxine]) may cause serotonin syn-
uric acid nephropathy, elderly pts, pts in drome. May increase concentration, tox-
third trimester of pregnancy, pts at high icity of tricyclic antidepressants (e.g.,
risk for suicide, family history of bipolar amitriptyline, doxepin). HERBAL:
disorder or mania, pts with risk factors Glucosamine, herbals with anti-
for QT prolongation (e.g., hypokalemia, coagulant/antiplatelet properties
hypomagnesemia), alcoholism. Pts in (e.g., garlic, ginger, ginkgo biloba,
whom weight loss is undesirable. ginseng) may increase concentration/
effect. FOOD: Grapefruit products may
ACTION increase concentration/effect. LAB VAL-
Blocks reuptake of the neurotransmitter UES: May increase total serum choles-
serotonin at CNS neuronal presynaptic terol, triglycerides, ALT, AST. May decrease
membranes, increasing availability at serum uric acid.

underlined – top prescribed drug


sertraline 1071

AVAILABILITY (Rx) throughout menstrual cycle or 100 mg/


Oral Concentrate: 20 mg/mL. Tab- day when dosing during luteal phase only.
lets: 25 mg, 50 mg, 100 mg.
Dosage in Renal Impairment
ADMINISTRATION/HANDLING No dose adjustment.
PO Dosage in Hepatic Impairment
• Give with food, milk if GI distress Use caution.
occurs. • Oral concentrate must be diluted
before administration. Mix with 4 oz water, SIDE EFFECTS
ginger ale, lemon/lime soda, or orange Frequent (26%–12%): Headache, nausea,
juice only. Give immediately after mixing. diarrhea, insomnia, drowsiness, dizzi-
ness, fatigue, rash, dry mouth. Occa-
INDICATIONS/ROUTES/DOSAGE sional (6%–4%): Anxiety, nervousness,
Depression agitation, tremor, dyspepsia, diaphoresis,
PO: ADULTS: Initially, 50 mg/day. May vomiting, constipation, sexual dysfunc-
increase by 25–50 mg/day at 7-day inter- tion, visual disturbances, altered taste.
vals up to 200 mg/day. ELDERLY: Initially, Rare (less than 3%): Flatulence, urinary
25 mg/day. May increase by 25–50 mg/ frequency, paresthesia, hot flashes, chills.
day at 7-day intervals up to 200 mg/day.
ADVERSE EFFECTS/
Obsessive-Compulsive Disorder (OCD) TOXIC REACTIONS
PO: ADULTS, CHILDREN 13–17 YRS: Ini-
Serotonin syndrome (seizures, arrhyth-
tially, 50 mg/day with morning or eve-
mias, high fever), neuroleptic malignant
ning meal. May increase by 25–50 mg/
syndrome (muscle rigidity, cognitive
day at 7-day intervals up to 200 mg/day.
changes), suicidal ideation have occurred.
ELDERLY, CHILDREN 6–12 YRS: Initially,
25 mg/day. May increase by 25–50 mg/ NURSING CONSIDERATIONS
day at 7-day intervals. Maximum: 200
mg/day. BASELINE ASSESSMENT
Assess appearance, behavior, speech pat-
Panic Disorder terns, level of interest, mood. For pts on
PO: ADULTS, ELDERLY: Initially, 25 mg long-term therapy, CBC, renal function,
once daily for 3–7 days. May increase LFT should be performed periodically.
to 50 mg/day. May further increase dose S
INTERVENTION/EVALUATION
based on response and tolerability in
increments of 25–50 mg at intervals of at Assess mental status for depression, sui-
least 1 wk. Maximum: 200 mg/day. cidal ideation (esp. at beginning of therapy
or change in dosage), anxiety, social func-
Post-Traumatic Stress Disorder (PTSD), tion, panic attack. Monitor daily pattern of
Social Anxiety Disorder (SAD) bowel activity, stool consistency. Assist with
PO: ADULTS, ELDERLY: Initially, 25–50 ambulation if dizziness occurs.
mg/day. May increase by 25–50 mg/day
PATIENT/FAMILY TEACHING
at 7-day intervals. Range: 50–200 mg/
day. Maximum: 200 mg/day. • Dry mouth may be relieved by sugarless
gum, sips of water. • Report headache,
Premenstrual Dysphoric Disorder (PMDD) fatigue, tremor, sexual dysfunc-
PO: ADULTS: Initially, 50 mg/day either tion. • Avoid tasks that require alertness,
daily throughout menstrual cycle or lim- motor skills until response to drug is estab-
ited to luteal phase of menstrual cycle. May lished (may cause dizziness, drowsi-
increase up to 150 mg/day per menstrual ness). • Take with food if nausea
cycle in 50-mg increments when dosing occurs. • Inform physician if pregnancy

Canadian trade name Non-Crushable Drug High Alert drug


1072 sevelamer
occurs. • Avoid alcohol. • Do not take INTERACTIONS
OTC medications without consulting physi- DRUG: May decrease concentration/effect
cian. • Report worsening of depression, of fluoroquinolones (e.g., levoFLOX-
suicidal ideation. acin), levothyroxine, mycophenolate.
HERBAL: None significant. FOOD: May
cause reduced absorption of vitamins D,
E, K, folic acid. LAB VALUES: Expected
sevelamer to decrease serum phosphate.
se-vel-a-mer AVAILABILITY (Rx)
(Renagel, Renvela) Powder for Oral Suspension:
Do not confuse Renagel with (Re­nvela): 0.8 g/pack, 2.4 g/pack.
Reglan, Regonol, or Renvela, or
Tablets: 800 mg.
sevelamer with Savella.
uCLASSIFICATION
ADMINISTRATION/HANDLING
PO
PHARMACOTHERAPEUTIC: Poly-
• Give with meals. • Space other medi-
meric phosphate binder. CLINICAL:
cation by at least 1 hr before or 3 hrs after
Electrolyte modifier, antihyperphos-
sevelamer. • Give tablets whole; do not
phatemia agent.
break, crush, dissolve, or divide. • Oral
Suspension: Mix 0.8 g with 30 mL water
USES (2.4 g with 60 mL water). Stir vigorously
Control of serum phosphorus in pts with to suspend (does not dissolve) just prior
chronic renal disease on hemodialysis. to drinking.

PRECAUTIONS INDICATIONS/ROUTES/DOSAGE
Hyperphosphatemia
Contraindications: Hypersensitivity to
sevelamer. Bowel obstruction. Cau- PO: ADULTS, ELDERLY: 800–1,600 mg
tions: Dysphagia, severe GI tract motility
with each meal, depending on severity
disorders, major GI tract surgery. of hyperphosphatemia (5.5–7.4 mg/
dL: 800 mg 3 times/day; 7.5–8.9 mg/
ACTION dL: 1,200–1,600 mg 3 times/day; 9
S Binds with phosphate within the intestinal mg/dL or greater: 1,600 mg 3 times/
lumen without altering calcium, aluminum, day). Maintenance: Based on serum
or bicarbonate concentration. Therapeu- phosphorus concentrations. Goal range:
tic Effect: Inhibits phosphate absorption. 3.5–5.5 mg/dL.
Decreases serum phosphate concentration. Serum Phosphorus
Concentration Dosage
PHARMACOKINETICS Greater than 5.5 Increase by 400–
Not absorbed systemically. Unknown if mg/dL 800 mg per meal
at 2-wk intervals
removed by hemodialysis. 3.5–5.5 mg/dL Maintain current
dosage
LIFESPAN CONSIDERATIONS Less than 3.5 mg/dL Decrease by 400–
Pregnancy/Lactation: Not distributed 800 mg per meal
in breast milk. Children: Safety and effi-
cacy not established. Elderly: No age-
Dosage in Renal/Hepatic Impairment
related precautions noted.
No dose adjustment.

underlined – top prescribed drug


simvastatin 1073

SIDE EFFECTS uCLASSIFICATION


Frequent (20%–11%): Infection, pain, hypo- PHARMACOTHERAPEUTIC: Hydrox-
tension, diarrhea, dyspepsia, nausea, vom- ymethylglutaryl-CoA (HMG-CoA)
iting. Occasional (10%–1%): Headache, reductase inhibitor. CLINICAL: Anti-
constipation, hypertension, increased hyperlipidemic.
cough.
ADVERSE EFFECTS/TOXIC USES
REACTIONS Secondary prevention of cardiovascular
Thrombosis occurs rarely. events in pts with hypercholesterolemia
and coronary heart disease (CHD) or at
NURSING CONSIDERATIONS high risk for CHD. Treatment of hyper-
BASELINE ASSESSMENT
lipidemias to reduce elevations in total
serum cholesterol, LDL-C, apolipoprotein
Obtain baseline chemistries, esp serum B, triglycerides, VLDL-C and increase
calcium, phosphate; assess for bowel HDL-C. Treatment of homozygous familial
obstruction. hypercholesterolemia (HoFH). Treatment
INTERVENTION/EVALUATION of heterozygous familial hypercholesterol-
Monitor serum phosphate, bicarbonate, emia (HeFH) in adolescents (10–17 yrs,
chloride, calcium. females more than 1 yr postmenarche).

PATIENT/FAMILY TEACHING PRECAUTIONS


• Take with meals, swallow tablets whole; Contraindications: Hypersensitivity to sim-
do not chew, crush, dissolve, or divide vastatin. Active hepatic disease or unex-
tablets. • Report persistent headache, plained, persistent elevations of hepatic
nausea, vomiting, diarrhea, hypotension. function test results, pregnancy, breast-
feeding, concurrent use of strong CYP3A4
inhibitors (e.g., clarithromycin, cyclo-
SPORINE, gemfibrozil). Cautions: History
simvastatin of hepatic disease, diabetes, severe renal
impairment, substantial alcohol consump-
sim-va-sta-tin tion. Withholding or discontinuing simvas-
(FloLipid, Zocor) tatin may be necessary when pt is at risk
Do not confuse simvastatin with for renal failure secondary to rhabdomy- S
atorvastatin, lovastatin, nystatin, olysis. Concomitant use of other medica-
pitavastatin, or pravastatin, tions associated with myopathy.
or Zocor with Cozaar, Lipitor,
Zoloft, or ZyrTEC. ACTION
Interferes with cholesterol biosynthesis
FIXED-COMBINATION(S) by inhibiting conversion of the enzyme
Juvisync: simvastatin/SITagliptin (an HMG-CoA to mevalonate. Therapeutic
antidiabetic agent): 10 mg/100 mg, Effect: Decreases LDL, cholesterol,
20 mg/100 mg, 40 mg/100 mg. Sim- VLDL, triglyceride levels; increase in HDL
cor: simvastatin/niacin (an antilipemic concentration.
agent): 20 mg/500 mg, 40 mg/500
mg, 20 mg/750 mg, 20 mg/1000 mg, PHARMACOKINETICS
40 mg/1000 mg. Vytorin: simvastatin/ Well absorbed from GI tract. Protein
ezetimibe (a cholesterol absorption in- binding: 95%. Metabolized in liver.
hibitor): 10 mg/10 mg, 20 mg/10 mg, Excreted in feces (60%), urine (13%).
40 mg/10 mg, 80 mg/10 mg. Unknown if removed by hemodialysis.

Canadian trade name Non-Crushable Drug High Alert drug


1074 simvastatin
Route Onset Peak Duration Prevention of Cardiovascular Events
PO (to reduce 3 days 14 days N/A PO: ADULTS, ELDERLY: 10–20 mg once
cholesterol) daily. Range: 5–40 mg/day.
Hyperlipidemias
LIFESPAN CONSIDERATIONS PO: ADULTS, ELDERLY: Initially, 10–20
Pregnancy/Lactation: Contraindicated mg once daily. Pts with CHD or CHD
in pregnancy (suppression of choles- risk equivalents: Initially, 40 mg/day.
terol biosynthesis may cause fetal toxic- Range: 5–40 mg/day.
ity), lactation. Risk of serious adverse
reactions in breastfeeding infants. Chil- Homozygous Familial
dren: Safety and efficacy not established Hypercholesterolemia (HoFH)
in children less than 10 yrs of age or in PO: ADULTS, ELDERLY: 40 mg once daily
premenarchal girls. Elderly: No age- in evening.
related precautions noted.
Heterozygous Familial
INTERACTIONS Hypercholesterolemia (HeFH)
DRUG: CycloSPORINE, Strong CYP3A4 PO: CHILDREN 10–17 YRS: 10 mg once
inhibitors (e.g., clarithromycin, daily in evening. May increase to 20
ketoconazole), amiodarone, calcium mg once daily after 6 wks. May further
channel blockers (e.g., dilTIAZem, increase to 40 mg once daily after addi-
verapamil), colchicine, fibrates, gemfi- tional 6 wks. Maximum dose: 40 mg/
brozil, niacin, ranolazine may increase day.
risk of acute renal failure, rhabdomyolysis. Dosing Adjustment with Medications
Strong CYP3A4 inducers (e.g., carBA- (CycloSPORINE, gemfibrozil): Do not
Mazepine, phenytoin, rifAMPin) may exceed 10 mg/day. (Amiodarone,
decrease concentration/effect. HERBAL: St. amLODIPine, ranolazine): Do not
John’s wort may decrease concentration. exceed 20 mg/day. (DilTIAZem, drone-
FOOD: Grapefruit products may increase
darone, verapamil): Do not exceed 10
concentration, toxicity. Red yeast rice mg/day. (Lomitapide): Reduce simvas-
contains 2.4 mg lovastatin per 600 mg tatin dose by 50% when initiating lomi-
rice. LAB VALUES: May increase serum tapide. Do not exceed 20 mg/day.
creatine kinase (CK), transaminase.
S Dosage in Renal Impairment
AVAILABILITY (Rx) CrCl less than 30 mL/min: Initially,
Oral Suspension: 20 mg/5 mL, 40 mg/5 mL. 5 mg/day.
Tablets: 5 mg, 10 mg, 20 mg, 40 mg, 80 mg.
Dosage in Hepatic Impairment
ADMINISTRATION/HANDLING Contraindicated with active hepatic disease.
PO
• Give without regard to food. • Admin- SIDE EFFECTS
ister in evening for maximum efficacy. Generally well tolerated. Side effects are
Shake suspension well for 20 sec before usually mild and transient. Occasional
administering. (3%–2%): Headache, abdominal pain/
cramps, constipation, upper respiratory
INDICATIONS/ROUTES/DOSAGE tract infection. Rare (less than 2%): Diar-
Note: Limit 80-mg dose to pts taking rhea, flatulence, asthenia, nausea/vomit-
simvastatin longer than 12 mos without ing, depression.
evidence of myopathy.

underlined – top prescribed drug


siponimod 1075

ADVERSE EFFECTS/TOXIC USES


REACTIONS Treatment of relapsing forms of multiple
Potential for ocular lens opacities. Hyper- sclerosis (MS), including clinically iso-
sensitivity reaction, hepatitis occur rarely. lated syndrome, relapsing-remitting dis-
Myopathy (muscle pain, tenderness, weak- ease, and active secondary progressive
ness with elevated serum creatine kinase disease, in adults.
[CK], sometimes taking the form of rhab-
domyolysis) has occurred. PRECAUTIONS
Contraindications: Hypersensitivity to
NURSING CONSIDERATIONS siponimod. Pts with CYP2C9*3/*3 geno-
BASELINE ASSESSMENT type. Recent (within 6 mos) MI, unstable
angina, CVA, TIA, decompensated HF
Obtain dietary history, esp. fat consump- requiring hospitalization, NYHA class III/
tion. Question for possibility of pregnancy IV HF. Sick sinus syndrome, Mobitz type II
before initiating therapy. Question for second- or third-degree AV block (unless
history of hypersensitivity to simvastatin. pt has functioning pacemaker). Cautions:
Assess baseline lab results: serum choles- Conditions predisposing to infection
terol, LDL, VLDL, HDL, triglycerides, LFT. (e.g., diabetes, immunocompromised
INTERVENTION/EVALUATION pts, renal failure, open wounds), baseline
Monitor serum cholesterol, triglyceride sinus bradycardia, severe hepatic impair-
lab results for therapeutic response. ment, hypertension, altered pulmonary
Monitor LFT. Monitor daily pattern of function, pts at risk for developing AV
bowel activity, stool consistency. Assess block (congenital heart disease, ischemic
for headache, myopathy. heart disease, HF), pts at risk for macular
edema (e.g., diabetes, history of uveitis);
PATIENT/FAMILY TEACHING history of syncope, thromboembolic
• Use appropriate contraceptive mea- events (CVA, pulmonary embolism, MI
sures. • Periodic lab tests are essential [more than 6 mos prior]). Concomitant
part of therapy. • Maintain appropriate use of antiarrhythmics, beta blockers,
diet. Avoid grapefruit products. • Report calcium channel blockers, immunosup-
unexplained muscle pain, tenderness, pressants, immune modulators, anti-
weakness. neoplastics, QT interval–prolonging
medications. Not recommended in pts
with severe active infection; history of S

siponimod cardiac arrest, cerebrovascular disease,


uncontrolled hypertension, or severe,
untreated sleep apnea unless approved
si-pon-i-mod by a cardiologist.
(Mayzent)
Do not confuse siponimod with ACTION
fingolimod. Blocks capacity of lymphocytes to move
uCLASSIFICATION out from lymph nodes, reducing the
number of lymphocytes available to the
PHARMACOTHERAPEUTIC: Sphingo- CNS. Therapeutic Effect: May involve
sine-1-phosphate receptor modu- reduction of lymphocyte migration into
lator. CLINICAL: Multiple sclerosis the CNS, reducing inflammation.
agent.
PHARMACOKINETICS
Widely distributed. Metabolized in liver.
Protein binding: 68%. Peak plasma

Canadian trade name Non-Crushable Drug High Alert drug


1076 siponimod
concentration: 4 hrs. Steady state dose. Do not use starter pack in pts who
reached in 6 days. Excreted primarily in titrate to 1 mg maintenance dose. • If
feces. Half-life: 30 hrs. one dose titration is missed for more
than 24 hrs, reinitiate treatment starting
LIFESPAN CONSIDERATIONS with day 1 of titration regimen. • If
Pregnancy/Lactation: Avoid pregnancy; treatment is interrupted for more than 4
may cause fetal harm. Female pts of consecutive days after initial titration is
reproductive potential should use effective completed, reinitiate treatment starting
contraception during treatment and up to with day 1 of titration regimen.
10 days after discontinuation. Unknown if
distributed in breast milk. Children: Safety INDICATIONS/ROUTES/DOSAGE
and efficacy not established. Elderly: Age- Multiple Sclerosis (Relapsing)
related hepatic impairment may increase PO: ADULTS, ELDERLY: (Pts with CYP2C9
risk of adverse effects/hepatic injury. genotypes *1/*1, *1/*2, or *2/*2):
0.25 mg on day 1, then 0.25 mg on day
INTERACTIONS 2, then 0.5 mg on day 3, then 0.75 mg on
DRUG: Beta blockers (e.g., carvedilol, day 4, then 1.25 mg on day 5. Mainte-
metoprolol), bretylium, calcium nance: 2 mg once daily starting on day 6.
channel blockers (e.g., dilTIAZem, (Pts with CYP2C9 genotypes *1/*3 or
verapamil), ceritinib, digoxin, *2/*3): 0.25 mg on day 1, then 0.25 mg
lacosamide may increase risk of AV on day 2, then 0.5 mg on day 3, then 0.75
block, bradycardia. May increase QT mg on day 4. Maintenance: 1 mg once
interval–prolonging effect of amio- daily starting on day 5.
darone, azithromycin, haloperidol.
May decrease therapeutic effect of BCG Dosage in Renal Impairment
(intravesical), live vaccines. May Mild to severe impairment: No dose
increase toxic effect of live vaccines. Flu- adjustment.
conazole may increase concentration/ Dosage in Hepatic Impairment
effect. RifAMPin may decrease concen- Mild to moderate impairment: No
tration/effect. May increase toxic effects dose adjustment. Severe impairment:
of denosumab, leflunomide, natali- Use caution.
zumab, tacrolimus. May decrease
therapeutic effect of nivolumab, sipu- SIDE EFFECTS
S leucel-T, tertomotide. May increase Occasional (15%–6%): Headache, hyper-
immunosuppressive effect of tofacitinib, tension, peripheral edema, nausea, diz-
other immunosuppressants. HERBAL: ziness, diarrhea, extremity pain.
Echinacea may decrease therapeutic
effect. FOOD: None known. LAB VALUES: ADVERSE EFFECTS/TOXIC
May increase serum ALT, AST, bilirubin, REACTIONS
GGT. Expected to cause a dose-dependent Life-threatening infections (bronchitis,
reduction in peripheral lymphocyte count sinusitis, upper respiratory tract infec-
to 20%–30% of baseline values. tion, fungal skin infection) reported in
3% of pts. Fatal cases of cryptococcal
AVAILABILITY (Rx) meningitis, disseminated cryptococcal
Tablets: 0.25 mg, 2 mg. infections were reported. Herpes zoster
infections reported in 5% of pts. Reacti-
ADMINISTRATION/HANDLING vation of herpes viral infection may cause
PO varicella zoster meningitis. Progressive
• Give without regard to multifocal leukoencephalopathy (PML),
meals. • Starter pack should be used in an opportunistic viral infection of the
pts who titrate to 2 mg maintenance brain caused by the JC virus, may result
underlined – top prescribed drug
siponimod 1077
in progressive permanent disability and (chickenpox) should be tested for antibod-
death. Posterior reversible encephalopa- ies prior to initiation. A full vaccination
thy syndrome, a dysfunction of the brain course for varicella in antibody-negative pts
that may evolve into an ischemic CVA or is recommended prior to initiation. Perform
cerebral hemorrhage, may occur. Macu- baseline ophthalmologic evaluation of the
lar edema reported in 2% of pts. Pts with fundus (including the macula) prior to ini-
diabetes or history of uveitis are at an tiation. Receive full medication history and
increased risk for developing macular screen for interaction (esp. immunosup-
edema. Bradycardia reported in 4% of pressants; drugs known to bradycardia, AV
pts. AV conduction delays reported in 5% conduction delay). Question history as listed
of pts. Dose-dependent reductions of pul- in Precautions. Screen for active infection.
monary function (absolute forced expira-
INTERVENTION/EVALUATION
tory volume over 1 sec) reported in 3%
of pts. Hepatic injury (transaminitis) At initial treatment (within first 4–6 hrs
reported in 10% of pts. Seizures reported after dose), therapy reduces heart rate,
in 2% of pts. Falls reported in 11% of AV conduction. In pts with preexisting
pts. Rebound or severe exacerbation cardiac conditions, monitor for symp-
of disease may occur after discontinua- tomatic bradycardia for at least 6 hrs after
tion. May increase risk of hypertension, first dose with hourly pulse, B/P, and then
new malignancies. Fatal thromboembolic obtain ECG at the end of day 1. If heart
events including CVA, pulmonary embo- rate is less than 45 beats/min, QTc inter-
lism, MI reported in 3% of pts. val is 500 msec or greater, or new-onset
second-degree (or higher) AV block is
NURSING CONSIDERATIONS present after 6 hrs of first dose, continue
monitoring until resolved. If intervention
BASELINE ASSESSMENT
is required, continue heart monitoring
Obtain CBC, LFT, ECG. Test all pts for overnight and repeat 6-hr monitoring
CYP2C9 variants to determine CYP2C9 after second dose. Conduct ophthalmic
genotype. examination with any change of vision.
Assess baseline symptoms of MS (e.g., Pts with altered mental status, seizures,
bladder/bowel dysfunction, cognitive im- visual disturbances, unilateral weakness
pairment, depression, dysphagia, fatigue, should be evaluated for cryptococcal
gait disorder, numbness/tingling, pain, meningitis, varicella zoster meningitis,
seizures, spasticity, tremors, weakness). posterior reversible encephalopathy syn- S
Consultation with a cardiologist is advised drome, PML. Persistent immunosuppres-
in pts with QT interval prolongation greater sive effects may occur for up to 3–4 wks
than 500 msec; arrhythmias requiring treat- after discontinuation. Closely monitor for
ment with Class Ia or Class III antiarrhyth- adverse effects if other immunosuppres-
mic; ischemic heart disease, HF, history of sants are initiated within the first 3–4 wks
cardiac arrest, recent MI; history of Mobitz after discontinuation. Monitor B/P for hy-
type II second- or third-degree AV block, pertension. Monitor for systemic or local
sick sinus syndrome, sinoatrial heart block. infections, herpetic infections; symptoms
First-dose monitoring is recommended of new malignancies. Conduct neurologic
in pts with preexisting cardiac conditions assessment. Assess for symptoms im-
(baseline sinus bradycardia, first- or sec- provement of MS. Monitor for symptoms
ond-degree [Mobitz type I], history of MI of MI (chest pain, diaphoresis, left arm/
[more than 6 mos prior], HF) in a medical jaw pain, increased serum troponin, ST
setting that can adequately treat symptom- segment elevation), CVA (aphasia, altered
atic bradycardia. Pts without a documented mental status, facial droop, hemiplegia,
history of vaccination against varicella zoster vision loss), pulmonary embolism (chest
or a confirmed history of varicella infection pain, dyspnea, tachycardia).

Canadian trade name Non-Crushable Drug High Alert drug


1078 sirolimus
PATIENT/FAMILY TEACHING
• Treatment may depress your immune sirolimus
system and reduce your ability to fight
infection. Report symptoms of infection sir-oh-li-mus
such as body aches, burning with urina- (Rapamune)
tion, chills, cough, fatigue, fever. Avoid j BLACK BOX ALERT jIncreased
those with active infection. • Any susceptibility to infection and
potential for development of
change of vision will require an immedi- lymphoma may result from immu-
ate eye examination. • PML, an oppor- nosuppression. Not recommended
tunistic viral infection of the brain, may for liver or lung transplant pts. Use
cause progressive, permanent disabilities only by physicians experienced in
or death. Report symptoms of PML such immunosuppressive therapy and
management of transplant pts.
as confusion, memory loss, paralysis, Do not confuse Rapamune
trouble speaking, vision loss, seizures, with Rapaflo, or sirolimus with
weakness. • Treatment may worsen everolimus, pimecrolimus,
high blood pressure or cause new can- tacrolimus, or temsirolimus.
cers. • Report liver problems (abdomi-
nal pain, bruising, clay-colored stool, uCLASSIFICATION
amber or dark colored urine, yellowing PHARMACOTHERAPEUTIC: mTOR
of the skin or eyes), lung problems kinase inhibitor. CLINICAL: Immu-
(reduced lung function, shortness of nosuppressant.
breath), heart arrhythmias (chest pain,
dizziness, fainting, palpitations, slow or
rapid heart rate, irregular heart USES
rate). • Posterior reversible encepha- Prophylaxis of organ rejection in pts
lopathy syndrome, a dysfunction of the receiving renal transplant (in com-
brain that may cause a stroke or bleeding bination with cycloSPORINE and
in the brain, may occur. • Treatment corticosteroids). Treatment of lymphan-
may cause life-threatening blood clots; gioleiomyomatosis. OFF-LABEL: Prophy-
report symptoms of heart attack (chest laxis of organ rejection in heart transplant
pain, difficulty breathing, jaw pain, nau- recipients. Prevention of acute graft-
sea, pain that radiates to the left arm, vs-host disease in allogeneic stem cell
sweating), lung embolism (difficulty transplantation. Treatment of refractory
S breathing, chest pain, rapid heart rate), acute or chronic graft-vs-host disease.
stroke (confusion, difficulty speaking, Rescue agent for acute and chronic organ
one-sided weakness or paralysis, loss of rejection.
vision). • Female pts of childbearing
potential must use effective contraception PRECAUTIONS
during treatment and for at least 10 days Contraindications: Hypersensitivity to siro-
after last dose. Do not breastfeed. • Due limus. Cautions: Cardiovascular disease
to high risk of interactions, do not take (HF, hypertension); pulmonary disease,
newly prescribed medications unless hepatic impairment, renal impairment,
approved by the provider who originally hyperlipidemia, perioperative period due
started treatment. • Do not receive live to increased chance of surgical compli-
vaccines for at least 4 wks after last cations from impaired wound and tissue
dose. • Severe worsening of MS symp- healing. Concurrent use with medications
toms may occur after stopping treatment. that may alter renal function.

underlined – top prescribed drug


sirolimus 1079

ACTION ADMINISTRATION/HANDLING
Inhibits T-lymphocyte activation and • Doses should be taken 4 hrs after cyclo-
proliferation in response to antigenic SPORINE. • Take consistently with or
and cytokine stimulation, and inhib- without food. • Do not break, crush, dis-
its antibody production. Therapeu- solve, or divide tablets. • Mix oral solu-
tic Effect: Inhibits acute rejection of tion with only water or orange juice, stir
allografts and prolongs graft survival. vigorously, drink immediately.
PHARMACOKINETICS INDICATIONS/ROUTES/DOSAGE
Rapidly absorbed from GI tract. Protein b ALERT c Tablets and oral solution
binding: 92%. Extensively metabolized in are not bioequivalent. (However, clinical
liver. Primarily excreted in feces (91%). equivalence shown at 2 mg dose.)
Half-life: 57–63 hrs.
Prevention of Organ Transplant Rejection
LIFESPAN CONSIDERATIONS (Low to Moderate Risk)
Pregnancy/Lactation: Unknown if drug PO: ADULTS, CHILDREN 13 YRS AND OLDER
crosses placenta or is distributed in breast WEIGHING MORE THAN 40 KG: Loading
milk. Children: Safety and efficacy not dose: 6 mg on day 1. Maintenance: 2
established in pts younger than 13 yrs. mg/day. ADULTS, CHILDREN 13 YRS AND
Elderly: No age-related precautions noted. OLDER WEIGHING LESS THAN 40 KG: Load-
ing dose: 3 mg/m2 on day 1. Mainte-
INTERACTIONS nance: 1 mg/m2/day.
DRUG: CYP3A4 inducers (e.g., car-
Prevention of Organ Transplant Rejection
BAMazepine, rifabutin, rifAMPin)
(High Risk)
may decrease concentration/effects.
PO: ADULTS: Loading dose: Up to 15
CYP3A4 inhibitors (e.g., clarithro-
mycin, erythromycin, itraconazole, mg on day 1. Maintenance: 5 mg/day.
verapamil) may increase concentra- Obtain trough between 5–7 days. Con-
tion, toxicity. May increase concentra- tinue therapy for 1 yr following trans-
tion/effects of cycloSPORINE (take plantation. Further adjustments based on
sirolimus 4 hrs after cycloSPORINE for clinical status.
renal transplant). May decrease the thera- Lymphangioleiomyomatosis
peutic effect; increase adverse effects of PO: ADULTS, ELDERLY: Initially, 2 mg/
vaccines (live). HERBAL: St. John’s S
day with dosage adjustment to maintain
wort may decrease concentration. Echi- concentration between 5–15 ng/mL.
nacea may decrease the therapeutic Obtain serum trough level after 10–20
effect. FOOD: Grapefruit products may days. Once maintenance dose is adjusted,
increase risk of myelotoxicity, nephrotox- further adjustments should be made at 7-
icity. LAB VALUES: May increase serum to 14-day intervals. Once a stable dose is
ALT, AST, alkaline phosphatase, LDH, BUN, attained, serum trough levels should be
creatine phosphate, cholesterol, triglyc- assessed at least q3mos.
erides, creatinine. May alter WBC, serum
glucose, calcium. May decrease Hgb, Hct. Dosage in Renal Impairment
No dose adjustment.
AVAILABILITY (Rx)
Oral Solution: 1 mg/mL. Dosage in Hepatic Impairment
Tablets: 0.5 mg, 1 mg, 2 mg. Loading dose: No change. Maintenance
dose: Mild to moderate impairment:
Reduce dose by 33%. Severe impair-
ment: Reduce dose by 50%.

Canadian trade name Non-Crushable Drug High Alert drug


1080 SITagliptin

SIDE EFFECTS or SITagliptin with SAXagliptin


Occasional: Hypercholesterolemia, or SUMAtriptan.
hyperlipidemia, hypertension, rash. High FIXED-COMBINATION(S)
doses (5 mg/day): Anemia, arthral-
gia, diarrhea, hypokalemia, peripheral Janumet, Janumet XR: SITagliptin/
edema, thrombocytopenia. metFORMIN (an antidiabetic): 50
mg/500 mg, 50 mg/1,000 mg.
ADVERSE EFFECTS/ uCLASSIFICATION
TOXIC REACTIONS
PHARMACOTHERAPEUTIC: DPP-4
Hepatotoxicity occurs rarely. Skin carci-
inhibitors (gliptins). CLINICAL: An-
noma (including basal cell, squamous
tidiabetic agent.
cell, melanoma) has been observed.
NURSING CONSIDERATIONS USES
BASELINE ASSESSMENT Adjunctive treatment to diet, exercise to
Obtain LFT. Assess for pregnancy, lac- improve glycemic control in pts with type
tation. Question for medication usage 2 diabetes as monotherapy or in combi-
(esp. cycloSPORINE, dilTIAZem, keto- nation with other antidiabetic agents.
conazole, rifAMPin). Determine if pt has PRECAUTIONS
chickenpox, herpes zoster, malignancy,
Contraindications: Hypersensitivity to
infection.
SITagliptin. Cautions: Type 1 diabetes, dia-
INTERVENTION/EVALUATION betic ketoacidosis, renal impairment, end-
Monitor serum renal function, LFT peri- stage renal disease, history of pancreatitis,
odically. Monitor serum cholesterol, tri- angioedema with other DPP-4 inhibitors.
glycerides, platelets; Hgb. Obtain trough Concurrent use of other glucose-lowering
concentration 10–20 days after dose. agents may increase risk of hypoglycemia.
Once maintenance dose is adjusted, ACTION
make further adjustments at intervals of
7–14 days. Once stable dose is attained, Inhibits DPP-4 enzyme, causing pro-
assess trough concentration at least longed active incretin levels. Incretin reg-
q3mos. ulates glucose homeostasis. Therapeutic
Effect: Regulates glucose homeostasis.
S PATIENT/FAMILY TEACHING Increases synthesis and release of insu-
• Avoid those with colds, other infections. lin from pancreatic cells; lowers gluca-
• Avoid grapefruit products. • Avoid gon secretion from pancreas, decreases
exposure to sunlight, artificial light hepatic glucose production.
sources. • Strict monitoring is essential
in identifying, preventing symptoms of PHARMACOKINETICS
organ rejection. • Do not chew, crush, Route Onset Peak Duration
dissolve, or divide tablets. PO N/A 1–4 hrs 24 hrs

Rapidly absorbed. Protein binding: 38%.


Excreted in urine (87%), feces (13%).
SITagliptin Half-life: 12 hrs.
sit-a-glip-tin LIFESPAN CONSIDERATIONS
(Januvia) Pregnancy/Lactation: Unknown if dis-
Do not confuse Januvia with tributed in breast milk. Children: Safety
Enjuvia, Jantoven, or Janumet, and efficacy not established. Elderly: No
age-related precautions noted.

underlined – top prescribed drug


sodium bicarbonate 1081

INTERACTIONS INTERVENTION/EVALUATION
DRUG: May enhance hypoglycemic effect of Monitor serum glucose, Hgb A1c, BUN,
insulin, sulfonylureas (e.g., glipiZIDE, creatinine. Assess for hypoglycemia
glyBURIDE). HERBAL: None significant. (diaphoresis, tremor, dizziness, anxiety,
FOOD: None known. LAB VALUES: May headache, tachycardia, perioral numb-
slightly increase WBCs, particularly neutro- ness, hunger, diplopia, difficulty concen-
phil count. May increase serum creatinine. trating), hyperglycemia (polyuria, poly-
phagia, polydipsia, nausea, vomiting, dim
AVAILABILITY (Rx) vision, fatigue, deep, rapid breathing).
Tablets, Film-Coated: 25 mg, 50 mg, Be alert to conditions that alter glucose
100 mg. requirements (fever, increased activity,
stress, trauma, surgical procedures).
ADMINISTRATION/HANDLING
PATIENT/FAMILY TEACHING
PO
• May give without regard to • Diabetes requires lifelong con-
food. • Do not break, crush, dissolve, trol. • Prescribed diet, exercise are
or divide film-coated tablets. principal part of treatment; do not skip,
delay meals. • Continue to adhere to
INDICATIONS/ROUTES/DOSAGE dietary instructions, regular exercise
Type 2 Diabetes program, regular testing of serum glu-
PO: ADULTS OVER 18 YRS, ELDERLY: 100 cose. • When taking combination drug
mg once daily. therapy or when glucose demands are
Dosage in Renal Impairment
altered (fever, infection, trauma, stress,
CrCl 30 mL/min to less than 50 mL/
heavy physical activity), have source of
min: 50 mg once daily. CrCl less than
glucose available to treat symptoms of
30 mL/min, ESRD, dialysis: 25 mg
hypoglycemia. • Report nausea, vomit-
once daily. ing, anorexia, severe abdominal pain,
pancreatitis.
Dosage in Hepatic Impairment
No dose adjustment.
SIDE EFFECTS sodium bicarbonate
Occasional (5% and greater): Headache,
nasopharyngitis. Rare (3%–1%): Diarrhea, soe-dee-um bye-kar-boe-nate S
abdominal pain, nausea. (Neut)
ADVERSE EFFECTS/TOXIC uCLASSIFICATION
REACTIONS
PHARMACOTHERAPEUTIC: Alkalin-
Hypersensitivity reactions including
izing agent. CLINICAL: Antacid, elec-
angioedema, Stevens-Johnson syndrome
trolyte supplement, urinary/systemic
reported. Acute pancreatitis occurs rarely.
alkalinizer.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT USES
Check serum glucose concentration be- Management of metabolic acidosis, gas-
fore administration. Assess renal func- tric hyperacidity. Alkalinization agent for
tion. Discuss lifestyle to determine extent urine; hyperkalemia treatment; manage-
of learning, emotional needs. Ensure ment of overdose of tricyclic antidepres-
follow-up instruction if pt, family do not sants and aspirin. OFF-LABEL: Prevention
thoroughly understand diabetes manage- of contrast-induced nephropathy.
ment, glucose-testing technique.

Canadian trade name Non-Crushable Drug High Alert drug


1082 sodium bicarbonate
PRECAUTIONS AVAILABILITY (Rx)
Contraindications: Hypersensitivity to 0.5 mEq/mL
Injection Solution (Rx):
sodium bicarbonate. Hypernatremia, (4.2%), 1 mEq/mL (8.4%). Tablets
alkalosis, unknown abdominal pain, (OTC): 325 mg, 650 mg.
hypocalcemia, severe pulmonary edema.
Cautions: HF, edematous states, renal ADMINISTRATION/HANDLING
insufficiency, cirrhosis. IV

ACTION b ALERT c For direct IV administration


Dissociates to provide bicarbonate ion. in neonates or infants, use 0.5 mEq/mL
Therapeutic Effect: Neutralizes hydro- concentration.
gen ion concentration, raises blood, uri- Reconstitution • May give undiluted.
nary pH. Rate of administration • For IV push,
give up to 1 mEq/kg over 1–3 min for
PHARMACOKINETICS cardiac arrest. • For IV infusion, do not
Route Onset Peak Duration exceed rate of infusion of 1 mEq/kg/
PO 15 min N/A 1–3 hrs hr. • For children younger than 2 yrs,
IV Immediate N/A 8–10 min premature infants, neonates, administer by
slow infusion, up to 10 mEq/min.
Well absorbed following PO administra- Storage • Store at room temperature.
tion, sodium bicarbonate dissociates
to sodium and bicarbonate ions. With PO
increased hydrogen ion concentrations, • Give 1–3 hrs after meals.
bicarbonate ions combine with hydrogen IV INCOMPATIBILITIES
ions to form carbonic acid, which then
dissociates to CO2, which is excreted by Amiodarone (Cordarone), ascorbic acid,
the lungs. Plasma concentration regu- calcium chloride, dilTIAZem (Cardizem),
lated by kidney (ability to form, excrete DOBUTamine (Dobutrex), DOPamine
bicarbonate). (Intropin), HYDROmorphone (Dilaudid),
magnesium sulfate, midazolam (Versed),
LIFESPAN CONSIDERATIONS norepinephrine (Levophed), ondansetron
Pregnancy/Lactation: May produce (Zofran).
hypernatremia, increase tendon reflexes IV COMPATIBILITIES
S in neonate or fetus whose mother is
administered chronically high doses. Dexmedetomidine (Precedex), furose-
May be distributed in breast milk. mide (Lasix), heparin, insulin, lidocaine,
Children: No age-related precautions mannitol, milrinone (Primacor), mor-
noted. Do not use as antacid in pts phine, phenylephrine (Neo-Synephrine),
younger than 6 yrs. Elderly: Age-related potassium chloride, propofol (Diprivan),
renal impairment may require dosage vancomycin (Vancocin).
adjustment. INDICATIONS/ROUTES/DOSAGE
INTERACTIONS b ALERT c May give by IV push, IV infu-
DRUG: May increase concentration, sion, or orally. Dose individualized based
toxicity of quiNIDine, quiNINE. May on severity of acidosis, laboratory values, pt
decrease effects of lithium. HERBAL: age, weight, clinical conditions. Do not fully
None significant. FOOD: Milk, other correct bicarbonate deficit during the first
dairy products may result in milk-alkali 24 hrs (may cause metabolic alkalosis).
syndrome. LAB VALUES: May increase
serum, urinary pH.

underlined – top prescribed drug


sodium chloride 1083
Cardiac Arrest SIDE EFFECTS
b ALERT c Routine use not recom- Frequent: Abdominal distention, flatu-
mended. lence, belching.
IV: ADULTS, ELDERLY: Initially, 1 mEq/kg.
May repeat based on arterial blood gases. ADVERSE EFFECTS/
CHILDREN, INFANTS: Initially, 0.5–1 mEq/ TOXIC REACTIONS
kg. May repeat based on arterial blood Excessive, chronic use may produce
gases. metabolic alkalosis (irritability, twitching,
paresthesia, cyanosis, slow or shallow res-
Metabolic Acidosis (Mild to Moderate) pirations, headache, thirst, nausea). Fluid
IV: ADULTS, ELDERLY, CHILDREN: 2–5 overload results in headache, weakness,
mEq/kg over 4–8 hrs. May repeat based blurred vision, behavioral changes, inco-
on acid-base status. ordination, muscle twitching, elevated B/P,
Prevention of Contrast-Induced bradycardia, tachypnea, wheezing, cough-
Nephropathy ing, distended neck veins. Extravasation
IV infusion: ADULTS, ELDERLY: 154 may occur at the IV site, resulting in tissue
mEq/L sodium bicarbonate in D5W solu- necrosis, ulceration.
tion: 3 mL/kg/hr 1 hr immediately before
contrast injection, then 1 mL/kg/hr dur- NURSING CONSIDERATIONS
ing contrast exposure and for 6 hrs after BASELINE ASSESSMENT
procedure.
Assess for signs and symptoms of acido-
Metabolic Acidosis (Associated with sis, alkalosis. Do not give PO medication
Chronic Renal Failure) within 1 hr of antacids.
PO: ADULTS, ELDERLY: Initially, 15.4–
INTERVENTION/EVALUATION
23.1 mEq/day in divided doses. Titrate to
normal serum bicarbonate level of 23–29 Monitor serum, urinary pH, CO2 level,
mEq/L. serum electrolytes, plasma bicarbonate
levels. Watch for signs of metabolic al-
Renal Tubular Acidosis (Distal) kalosis, fluid overload. Assess for clini-
PO: ADULTS, ELDERLY: 0.5–2 mEq/kg/ cal improvement of metabolic acidosis
day in 4–6 divided doses. CHILDREN: 2–3 (relief from hyperventilation, weakness,
mEq/kg/day in divided doses. disorientation). Monitor daily pattern of
bowel activity, stool consistency. Moni- S
Renal Tubular Acidosis (Proximal) tor serum phosphate, calcium, uric
PO: ADULTS, ELDERLY, CHILDREN: 5–10 acid levels. Assess for relief of gastric
mEq/kg/day in divided doses. Mainte- distress.
nance dose to maintain serum bicarbon-
ate in normal range.
Urine Alkalinization sodium chloride
PO: ADULTS, ELDERLY: Initially, 4 g, then
1–2 g q4h. Maximum: 16 g/day (8 g/ so-dee-um klor-ide
day in adults older than 60 yrs). (Muro 128, Nasal Moist, Ocean,
SalineX)
Antacid
PO: ADULTS, ELDERLY: 300 mg–2 g 1–4 uCLASSIFICATION
times/day. PHARMACOTHERAPEUTIC: Electro-
lyte supplement. CLINICAL: Elec-
Hyperkalemia trolyte, isotonic volume expander,
IV: ADULTS, ELDERLY: 50 mEq over 5 min. ophthalmic adjunct.

Canadian trade name Non-Crushable Drug High Alert drug


1084 sodium chloride

USES Ointment (OTC): (Muro 128): 5%. Ophthal-


Parenteral: Source of hydration; pre- mic Solution (OTC): (Muro 128): 2%, 5%.
vention/treatment of sodium, chloride Tablets (OTC): 1 g.
deficiencies (hypertonic for severe defi-
ciencies). Prevention of muscle cramps, ADMINISTRATION/HANDLING
heat prostration occurring with excessive IV
perspiration. Nasal: Restores moisture,
relieves dry, inflamed nasal membranes. • Hypertonic solutions (3% or 5%) are
Ophthalmic: Therapy in reduction of administered via large vein; avoid infiltra-
corneal edema, diagnostic aid in oph- tion; do not exceed 100 mL/hr. • Vials
thalmoscopic exam. containing 2.5–4 mEq/mL (concentrated
NaCl) must be diluted with D5W or D10W
PRECAUTIONS before administration.
Contraindications: Hypersensitivity to PO
so­dium chloride. Fluid retention, hyperna- • Do not crush/break enteric-coated or
tremia, hypertonic uterus. Cautions: HF, extended-release tablets. • Administer
renal impairment, cirrhosis, hyperten- with full glass of water.
sion, edema. Do not use sodium chloride
preserved with benzyl alcohol in neonates. Nasal
• Instruct pt to begin inhaling slowly just
ACTION before releasing medication into nose.
Sodium is a major cation of extracellu- • Instruct pt to inhale slowly, then
lar fluid. Therapeutic Effect: Controls release air gently through mouth. • Con-
water distribution, fluid and electrolyte tinue technique for 20–30 sec.
balance, osmotic pressure of body fluids;
Ophthalmic
maintains acid-base balance.
• Place gloved finger on lower eyelid
PHARMACOKINETICS and pull out until pocket is formed
Well absorbed from GI tract. Widely dis- between eye and lower lid. • Place pre-
tributed. Primarily excreted in urine and, scribed number of drops (or ¼–½ inch
to a lesser degree, in sweat, tears, saliva. of ointment) into pocket. • Instruct pt
to close eye gently for 1–2 min so that
LIFESPAN CONSIDERATIONS medication will not be squeezed out of
S Pregnancy/Lactation: No precautions sac. • When lower lid is released, have
noted. Children/Elderly: No age- pt keep eye open without blinking for at
related precautions noted. least 30 sec for solution; for ointment,
have pt close eye, roll eyeball around to
INTERACTIONS distribute medication. • When using
DRUG: May decrease effect of lithium. drops, apply gentle finger pressure to
May enhance adverse/toxic effects lacrimal sac at inner canthus for 1 min to
of tolvaptan. HERBAL: None significant. minimize systemic absorption.
FOOD: None known. LAB VALUES: None
significant. INDICATIONS/ROUTES/DOSAGE
b ALERT c Dosage based on age,
AVAILABILITY (Rx) weight, clinical condition; fluid, electro-
Injection Concentrate (Rx): 23.4% (4 lyte, acid-base balance status.
mEq/mL). Injection Solution (Rx): 0.45%,
Usual Parenteral Dosage
0.9%, 3%. Irrigation (Rx): 0.45%, 0.9%.
Nasal Gel (OTC): (Nasal Moist): 0.65%.
Deter-
IV: ADULTS, ELDERLY, CHILDREN:
Nasal Solution (OTC): (SalineX): 0.4%
mined by laboratory determinations
(Nasal Moist, Ocean): 0.65%. Ophthalmic

underlined – top prescribed drug


sofosbuvir/velpatasvir 1085
(mEq). Dosage varies widely based on
clinical conditions. sofosbuvir/
Usual Oral Dosage velpatasvir
PO: ADULTS, ELDERLY: 1–2 g 3 times/day.
soe-fos-bue-vir/vel-pat-as-vir
Usual Nasal Dosage (Epclusa)
Intranasal: ADULTS, ELDERLY, CHIL- Do not confuse sofosbuvir
DREN: 2–3 sprays as needed. with boceprevir, dasabuvir,
Usual Ophthalmic Dosage fosamprenavir, or simeprevir,
Ophthalmic solution: ADULTS, ELDERLY: or velpatasvir with daclatasvir,
Apply 1–2 drops q3–4h. grazoprevir, or paritaprevir.
Ophthalmic ointment: ADULTS, ELDERLY:
uCLASSIFICATION
Apply once daily or as directed.
PHARMACOTHERAPEUTIC: Nucleo-
SIDE EFFECTS tide analog NS5B polymerase inhibitor,
Frequent: Facial flushing. Occasional: NS5A inhibitor. CLINICAL: Antiviral.
Fever; irritation, phlebitis, extravasation
at injection site. Ophthalmic: Tempo-
rary burning, irritation. USES
Treatment of chronic hepatitis C virus
ADVERSE EFFECTS/ (HCV) genotype 1, 2, 3, 4, 5, or 6 infec-
TOXIC REACTIONS tion in adult pts without cirrhosis, or with
Too-rapid administration may produce compensated cirrhosis, or in combina-
peripheral edema, HF, pulmonary edema. tion with ribavirin in pts with decompen-
Excessive dosage may produce hypokale- sated cirrhosis.
mia, hypervolemia, hypernatremia.
PRECAUTIONS
NURSING CONSIDERATIONS Contraindications: Hypersensitivity to
BASELINE ASSESSMENT sofosbuvir, velpatasvir. If given with
Obtain baseline serum electrolyte studies. ribavirin, contraindications to ribavirin
Assess fluid balance (I&O, daily weight, apply. Cautions: Anemia (when used
lung sounds, edema). with ribavirin), renal impairment, end-
stage renal disease requiring hemodi-
INTERVENTION/EVALUATION alysis, hepatic disease unrelated to HCV S
Monitor fluid balance (I&O, daily weight, infection, HIV infection. Concomitant
lung sounds, edema), IV site for extravasa- use of amiodarone (with or without beta
tion. Monitor serum electrolytes, acid-base blockers) in pts with underlying car-
balance, B/P. Hypernatremia associated diac disease. Concomitant use of P-gly-
with edema, weight gain, elevated B/P; hy- coprotein inducers, moderate CYP2B6
ponatremia associated with muscle cramps, inducers, strong CYP2C8 inducers,
nausea, vomiting, dry mucous membranes. moderate or strong CYP3A4 inducers not
recommended.
PATIENT/FAMILY TEACHING
• Temporary burning, irritation may ACTION
occur upon instillation of eye medica- Sofosbuvir inhibits the HCV NS5B RNA-
tion. • Discontinue eye medication and dependent RNA polymerase. Velpatasvir
report if severe pain, headache, rapid inhibits the VCV NS5A protein. Thera-
change in vision (peripheral, direct), peutic Effect: Inhibits viral replication
sudden appearance of floating spots, of HCV.
acute redness of eyes, pain on exposure
to light, double vision occurs.
Canadian trade name Non-Crushable Drug High Alert drug
1086 sofosbuvir/velpatasvir

PHARMACOKINETICS ADMINISTRATION/HANDLING
Rapidly absorbed following oral PO
administration. Widely distributed. • Give without regard to food.
Metabolized in liver. Protein binding:
sofosbuvir: 61%–68%; velpatasvir: INDICATIONS/ROUTES/DOSAGE
greater than 99.5%. Peak plasma con- Hepatitis C Virus Infection
centration: sofosbuvir: 0.5–1 hr; velpa- PO: ADULTS, ELDERLY: 1 tablet (sofos-
tasvir: 3 hrs. Excretion: sofosbuvir: urine buvir/velpatasvir) once daily.
(80%), feces (14%); velpatasvir: feces
(94%), urine (0.4%). Half-life: sofos- Treatment Regimen and Duration
buvir: 0.5 hr; velpatasvir: 15 hrs. Pts without cirrhosis or pts with
compensated cirrhosis (Child-Pugh
LIFESPAN CONSIDERATIONS A): 1 tablet once daily for 12 wks.
Pregnancy/Lactation: When used with Pts with decompensated cirrhosis
ribavirin, therapy is contraindicated (Child-Pugh B or C): 1 tablet once
in pregnant women and in men whose daily with ribavirin for 12 wks.
female partners are pregnant. Female and
Dosage in Renal Impairment
male pts of reproductive potential must
use effective contraception for at least 6 Mild to moderate impairment: CrCl
mos following discontinuation (if therapy greater than or equal to 30 mL/
includes ribavirin). Unknown if distrib- min: No dose adjustment. Severe
impairment: CrCl less than 30 mL/
uted in breast milk. Children: Safety
and efficacy not established. Elderly: No min, end-stage renal disease: Not
age-related precautions noted. specified; use caution.
Dosage in Hepatic Impairment
INTERACTIONS
Mild to severe impairment: No dose
DRUG: Moderate or potent induc- adjustment.
ers of CYP2B6, CYP2C8, CYP3A4,
P-glycoprotein (e.g., carBAMaze- SIDE EFFECTS
pine, phenytoin, OXcarbazepine, Frequent (22%–15%): Headache, fatigue.
rifampicin) may decrease concentra- Occasional (9%–5%): Nausea, asthenia,
tion/effect of sofosbuvir/velpatasvir. insomnia, irritability. Rare (2%): Rash.
Amiodarone (with or without beta
S blockers [e.g., carvedilol, meto- ADVERSE EFFECTS/
prolol]) may significantly increase risk TOXIC REACTIONS
of symptomatic bradycardia. Proton Symptomatic bradycardia requiring pace-
pump inhibitors (e.g., omepra- maker intervention was reported in pts
zole, pantoprazole) may decrease taking amiodarone and sofosbuvir, in com-
concentration/effect. HERBAL: None bination with daclatasvir or simeprevir.
significant. FOOD: None known. LAB Cardiac arrest was reported in a pt taking
VALUES: May increase serum biliru- amiodarone in combination with sofos-
bin (indirect), creatine phosphokinase buvir and ledipasvir. Bradycardia usually
(CPK), lipase. occurred within hrs to days, but may occur
AVAILABILITY (Rx) up 2 wks after initiation (when used with
amiodarone). Pts with underlying cardiac
Tablets, Fixed-Dose: sofosbuvir 400 mg/ disease or advanced hepatic disease or
velpatasvir 100 mg. taking concomitant beta blockers are at an
increased risk for bradycardia when used
concomitantly with amiodarone. Depres-
sion reported in 1% of pts.

underlined – top prescribed drug


sofosbuvir/velpatasvir/voxilaprevir 1087
treatment. • Do not take herbal prod-
NURSING CONSIDERATIONS ucts. • Avoid alcohol. • Maintain proper
BASELINE ASSESSMENT nutritional intake.
Obtain CBC (when used with ribavirin),
renal function test, LFT, HCV-RNA level; se-
rum lipase, CPK; pregnancy test in female sofosbuvir/velpatas-
pts of reproductive potential. Confirm
hepatitis C virus genotype. Question history vir/voxilaprevir
of renal impairment, hepatic disease unre-
lated to HCV infection; HIV infection or use soe-fos-bue-vir/vel-pat-as-vir/vox-i-
of antiretroviral therapy. Receive full medi- la-pre-vir
cation history, and screen for interactions (Vosevi)
(esp. concomitant use of amiodarone). j BLACK BOX ALERT j Test
all pts for hepatitis B virus (HBV)
INTERVENTION/EVALUATION infection prior to initiation. HBV
reactivation was reported in HBV/
Monitor serum lipase, CPK. Periodically HBC co-infected pts who were
monitor HCV-RNA level for treatment ef- undergoing or had completed treat-
fectiveness. If unable to discontinue amio- ment with HCV direct-acting anti-
darone, recommend inpatient cardiac virals and were not receiving HBV
monitoring for at least 48 hrs, followed by antiviral therapy. HBV reactivation
may cause fulminant hepatitis,
outpatient or self-monitoring of HR for at hepatic failure, and death.
least 2 wks after initiation. Cardiac monitor- Do not confuse sofosbuvir
ing is also recommended in pts who discon- with boceprevir, dasabuvir, or
tinue amiodarone just prior to initiation. simeprevir; or velpatasvir with
Reinforce birth control compliance and ob- daclatasvir, grazoprevir, or
tain monthly ­pregnancy tests in female pts of paritaprevir; or voxilaprevir
reproductive potential taking concomitant with boceprevir, grazoprevir, or
ribavirin. Encourage nutritional intake. paritaprevir.
PATIENT/FAMILY TEACHING
uCLASSIFICATION
• Pts who take amiodarone during therapy
PHARMACOTHERAPEUTIC: NS5A in-
may require inpatient and outpatient car-
hibitor, polymerase inhibitor, NS3/4A
diac monitoring (and in some cases, pace-
inhibitor, NS5B RNA polymerase in-
maker implantation) due to an increased S
hibitor. CLINICAL: Antihepaciviral.
risk of slow heartbeats or cardiac arrest. If
amiodarone cannot be interrupted or dis-
continued, immediately report symptoms of USES
slow heartbeat such as chest pain, confu- Treatment of adults with chronic hepatitis
sion, dizziness, fainting, light-headedness, C virus (HCV) infection without cirrhosis
memory problems, palpitations, weak- or with compensated cirrhosis who have
ness. • Treatment may be used in combi- genotype 1, 2, 3, 4, 5, or 6 infection and
nation with ribavirin. Inform pt of have previously been treated with an HCV
contraindications/adverse effects of ribavi- regimen containing an NS5A inhibitor or
rin therapy. If therapy includes ribavirin, who have genotype 1a or 3 infection and
female pts of reproductive potential should have previously been treated with an HCV
avoid pregnancy during treatment and up to regimen containing sofosbuvir without an
6 mos after last dose. • Immediately NS5A inhibitor.
report suspected pregnancy. • Do not
breastfeed. • Do not take newly pre-
scribed medications unless approved by
prescriber who originally started

Canadian trade name Non-Crushable Drug High Alert drug


1088 sofosbuvir/velpatasvir/voxilaprevir

PRECAUTIONS rifAMPin), tipranavir/ritonavir may


Contraindications: Hypersensitivity to decrease concentration/effects. Moder-
sofosbuvir, velpatasvir, voxilaprevir. Con- ate or potent inducers of CYP2B6,
comitant use of rifAMPin. Cautions: Mod- CYP2C8, CYP3A4, P-glycoprotein
erate to severe hepatic impairment, HIV (e.g., carBAMazepine, phenytoin,
infection. Concomitant use of amioda- oxycarbazepine, rifampicin) may
rone, beta blockers. Pts with underlying decrease concentration/effect. May
cardiac disease and/or liver disease may increase concentration/effect of rosu-
increase risk of bradycardia. Concomitant vastatin. Proton pump inhibitors
use of P-glycoprotein inducers, moderate (e.g., lansoprazole, pantoprazole)
or strong CYP2C8 inducers, moderate or may decrease concentration/effect.
strong CYP3A4 inducers not recommended. HERBAL: None significant. FOOD: None
known. LAB VALUES: May increase
ACTION serum bilirubin, creatine kinase, lipase.
Sofosbuvir inhibits the HCV NS5B RNA-
AVAILABILITY (Rx)
dependent RNA polymerase, velpatasvir
inhibits the HCV NS5A protein, voxilapre- 400
Tablets, Fixed-Dose Combination:
vir inhibits the NS3/4A protease, necessary mg (sofosbuvir)/100 mg (velpatas-
for proteolytic cleavage of HCV-encoded vir)/100 mg (voxilaprevir).
polyprotein. Therapeutic Effect: Inhib-
ADMINISTRATION/HANDLING
its viral replication of hepatitis C virus.
PO
PHARMACOKINETICS • Give with food.
Widely distributed. Metabolized in liver.
INDICATIONS/ROUTES/DOSAGE
Protein binding: sofosbuvir: 61%–65%;
velpatasvir: greater than 99.5%; voxi- Note: For pts with genotype 3 infection with
laprevir: greater than 99%. Peak plasma prior NS5A inhibitor failure and cirrhosis,
concentration: sofosbuvir: 2 hrs; velpa- concomitant ribavirin should be used.
tasvir: 4 hrs; voxilaprevir: 4 hrs. Excreted
Hepatitis C Virus Infection
in sofosbuvir: urine (80%), feces (14%);
PO: ADULTS, ELDERLY: 1 tablet (sofosbu-
velpatasvir: feces (94%), urine (0.4%);
vir/velpatasvir/voxilaprevir) once daily
voxilaprevir: primarily in feces. Half-
for 12 wks.
life: sofosbuvir: 0.5 hrs; velpatasvir: 17
S hrs; voxilaprevir: 33 hrs. Dosage in Renal Impairment
Mild to moderate impairment: No
LIFESPAN CONSIDERATIONS dose adjustment. Severe impairment,
Pregnancy/Lactation: Unknown if dis- ESRD: Not recommended due to higher
tributed in breast milk. Children: Safety exposure of sofosbuvir.
and efficacy not established. Elderly: No
age-related precautions noted. Dosage in Hepatic Impairment
Mild impairment: No dose adjust-
INTERACTIONS ment. Moderate to severe impair-
DRUG: Amiodarone may increase risk ment: Not recommended due to higher
of symptomatic bradycardia. Alumi- exposure of voxilaprevir.
num- or magnesium-containing ant-
acids, H2-receptor antagonists (e.g., SIDE EFFECTS
famotidine), proton pump inhibi- Frequent (21%–13%): Headache, fatigue,
tors (e.g., omeprazole) may decrease diarrhea, nausea. Occasional (6%–1%):
concentration/effect. Anticonvulsants Asthenia, insomnia, rash.
(e.g., carBAMazepine, phenytoin),
antimycobacterials (e.g., rifabutin,
underlined – top prescribed drug
solifenacin 1089

ADVERSE EFFECTS/TOXIC PATIENT/FAMILY TEACHING


REACTIONS • Pts who take amiodarone (an antiar-
HBV reactivation was reported in pts rhythmic) during therapy may require
co-infected with HBV/HVC; may result inpatient and outpatient cardiac monitor-
in fulminant hepatitis, hepatic failure, ing (and in some cases, pacemaker
death. Cardiac arrest, symptomatic bra- implantation) due to an increased risk of
dycardia, pacemaker implantation were slow heart rate or cardiac arrest. If amio-
reported in pts taking concomitant ami- darone therapy cannot be withheld or
odarone. Bradycardia usually occurred stopped, immediately report symptoms
within hrs to days, but may occur up to of slow heart rate such as chest pain,
2 wks after initiation. Pts with underly- confusion, dizziness, fainting, light-head-
ing cardiac disease, advanced hepatic edness, memory problems, palpitations,
disease, or pts taking concomitant beta weakness. • There is a high risk of
blockers are at an increased risk for drug interactions with other medications.
bradycardia when used concomitantly Do not take newly prescribed medica-
with amiodarone. Psychiatric disor- tions unless approved by prescriber who
ders including depression may occur. originally started treatment. • Do not
Angioedema, blistering skin rashes may take herbal products. • Avoid alcohol.
occur. • Report signs of depression.

NURSING CONSIDERATIONS
BASELINE ASSESSMENT solifenacin
Obtain renal function test, LFT, HCV-
RNA level; serum lipase, CPK; pregnancy sol-i-fen-a-sin
test in females of reproductive poten- (VESIcare)
tial. Confirm hepatitis C virus genotype. uCLASSIFICATION
Question history of renal impairment,
hepatic disease unrelated to HCV in- PHARMACOTHERAPEUTIC: Anticho-
fection; HIV infection; concomitant linergic agent, muscarinic receptor
use of antiretroviral therapy. Receive antagonist. CLINICAL: Urinary anti-
full medication history and screen for spasmodic.
interactions (esp. concomitant use of
amiodarone). S
USES
INTERVENTION/EVALUATION Treatment of overactive bladder with
Monitor serum lipase, CK. Periodically symptoms of urinary frequency, urgency,
monitor HCV-RNA level for treatment ef- or urge incontinence.
fectiveness. If unable to discontinue amio- PRECAUTIONS
darone, recommend inpatient cardiac
monitoring for at least 48 hrs, followed Contraindications: Hypersensitivity to soli-
by outpatient or self-monitoring of HR fenacin. Gastric retention, uncontrolled
for at least 2 wks after initiation. Cardiac narrow-angle glaucoma, urinary reten-
monitoring is also recommended in pts tion. Cautions: Bladder outflow obstruc-
who discontinue amiodarone just prior tion, GI obstructive disorders, decreased
to initiation. Encourage nutritional intake. GI motility, controlled narrow-angle
Monitor for new-onset or worsening of glaucoma, renal/hepatic impairment,
depression. congenital or acquired QT prolongation,
concurrent medications that prolong QT
interval, hypokalemia, hypomagnesemia,
hot weather and/or exercise.
Canadian trade name Non-Crushable Drug High Alert drug
1090 somatropin
ACTION Dosage in Renal/Hepatic Impairment
Severe renal impairment (CrCl
Inhibits muscarinic receptors. Thera-
less than 30 mL/min) or moderate
peutic Effect: Decreases urinary blad-
hepatic impairment: Maximum dos-
der contractions, increases residual
urine volume, decreases detrusor muscle age is 5 mg/day. Not recommended in
pressure. severe hepatic impairment.

PHARMACOKINETICS SIDE EFFECTS


Frequent (28%–13%): Dry mouth, con-
Well absorbed. Protein binding: 98%.
Metabolized in liver. Excreted in urine stipation. Occasional (5%–3%): Blurred
(69%), feces (23%). Half-life: 40–68 vision, UTI, dyspepsia, nausea. Rare (2%–
1%): Dizziness, dry eyes, fatigue, depres-
hrs.
sion, edema, hypertension, epigastric
LIFESPAN CONSIDERATIONS pain, vomiting, urinary retention.
Pregnancy/Lactation: Unknown if ADVERSE EFFECTS/TOXIC
drug crosses placenta or is distributed REACTIONS
in breast milk. Children: Safety and effi-
cacy not established. Elderly: No age- Angioneurotic edema, GI obstruction
related precautions noted. occur rarely. Overdose can result in
severe anticholinergic effects.
INTERACTIONS
NURSING CONSIDERATIONS
DRUG: CYP3A4 inhibitors (e.g.,
ketoconazole, erythromycin, azole BASELINE ASSESSMENT
antifungals, clarithromycin) may Assess symptoms of overactive bladder
increase concentration/effect. Acli- before beginning the drug. Question medi-
dinium, ipratropium, tiotropium, cal history as listed in Precautions. Screen
umeclidinium may increase anticholin- for concomitant medications known to
ergic effect. Strong CYP3A4 inducers prolong QT interval. Obtain baseline ECG.
(e.g., carBAMazepine, phenytoin,
rifAMPin) may decrease concentra- INTERVENTION/EVALUATION
tion/effect. HERBAL: St. John’s wort Monitor I&O, anticholinergic effects, cre-
may decrease concentration/effect. atinine clearance. Assess for decrease in
FOOD: Grapefruit products may symptoms. Obtain bladder scan if urinary
S increase concentration/effect. LAB VAL- retention is suspected.
UES: None known.
PATIENT/FAMILY TEACHING
AVAILABILITY (Rx) • Avoid tasks requiring alertness, motor
Tablets: 5 mg, 10 mg. skills until response to drug is esta­
blished. • Anticholinergic side effects
ADMINISTRATION/HANDLING include constipation, urinary retention,
PO blurred vision, heat prostration in hot envi-
• Give without regard to food. Swallow ronment. • Use caution during exercise,
tablets whole, with liquids. exposure to heat.

INDICATIONS/ROUTES/DOSAGE
Overactive Bladder somatropin
PO: ADULTS, ELDERLY: 5 mg/day; if toler-
ated, may increase to 10 mg/day. soe-ma-troe-pin
(Genotropin, Genotropin Miniquick,
Dosage with Potent CYP3A4 Inhibitors Humatrope, Norditropin FlexPro,
Maximum: 5 mg/day.

underlined – top prescribed drug


somatropin 1091
Nutropin, Nutropin AQ NuSpin, stimulating erythropoietin. Influences
­Omnitrope, Saizen, Serostim, metabolism of carbohydrates (decreases
Zomacton, ­Zorbtive) insulin sensitivity), fats (mobilizes fatty
Do not confuse somatropin with acids), minerals (retains phosphorus,
SUMAtriptan. sodium, potassium by promotion of cell
growth), proteins (increases protein syn-
uCLASSIFICATION thesis). Therapeutic Effect: Stimulates
PHARMACOTHERAPEUTIC: Polypep- growth.
tide hormone. CLINICAL: Growth
hormone. PHARMACOKINETICS
Well absorbed after SQ, IM administra-
tion. Localized primarily in kidneys, liver.
USES Half-life: IV: 20–30 min; SQ, IM: 3–5
Adults: Growth deficiency due to pitu- hrs.
itary disease, hypothalamic disease,
surgery, radiation, or trauma. Serostim: LIFESPAN CONSIDERATIONS
AIDS-related wasting or cachexia. Zorb- Pregnancy/Lactation: Unknown if
tive: Short bowel syndrome. Children: drug is distributed in breast milk. Chil-
Long-term treatment of growth failure dren/Elderly: No age-related precau-
due to lack of or inadequate endogenous tions noted.
growth hormone secretion; chronic renal
insufficiency; short stature, Turner’s INTERACTIONS
syndrome, Prader-Willi syndrome, or DRUG: Corticosteroids (e.g., hydro-
homeobox gene deficiency; idiopathic cortisone, predniSONE) may inhibit
short stature. OFF-LABEL: Treatment of growth response. Oral estrogens
pediatric HIV pts with wasting/cachexia; may decrease response to somatropin.
HIV adipose redistribution syndrome. HERBAL: None significant. FOOD: None
known. LAB VALUES: May increase
PRECAUTIONS serum alkaline phosphatase, inorganic
Contraindications: Hypersensitivity to phosphorus, parathyroid hormone. May
growth hormone. Pts with Prader-Willi decrease glucose tolerance. May slightly
syndrome with growth hormone defi- decrease thyroid function.
ciency who are severely obese or have
severe respiratory impairment, Prader- AVAILABILITY (Rx) S
Willi syndrome without growth hor- Injection, Powder for Reconstitution:
mone deficiency, children with closed (Genotropin): 5 mg, 12 mg. (Genotropin
epiphyses, acute critical illness due Miniquick): 0.2 mg, 0.4 mg, 0.6 mg, 0.8
to complications after open heart or mg, 1 mg, 1.2 mg, 1.4 mg, 1.6 mg, 1.8 mg,
abdominal surgery, multiple accidental 2 mg. (Omnitrope): 5.8 mg. (Saizen): 5 mg,
trauma, acute respiratory failure, active 8.8 mg. (Serostim): 4 mg, 5 mg, 6 mg.
neoplasia, diabetic retinopathy. Active (Zomacton): 5 mg, 10 mg. (Zorbtive): 8.8
malignancy, progression of active grow- mg. Injection Solution: (Omnitrope): 5
ing intracranial lesion or tumor. Cau- mg/1.5 mL, 10 mg/1.5 mL. (Norditropin
tions: Diabetes, elderly pts. FlexPro Pen): 5 mg/1.5 mL, 10 mg/1.5 mL,
30 mg/3 mL. (Nutropin AQ NuSpin): 5 mg/2
ACTION mL, 10 mg/2 mL, 20 mg/2 mL.
Stimulates cartilaginous growth areas
of long bones; increases number, size ADMINISTRATION/HANDLING
of skeletal muscle cells; influences b ALERT c Neonate: Benzyl alcohol
size of organs; increases RBC mass by as a preservative has been associated

Canadian trade name Non-Crushable Drug High Alert drug


1092 somatropin
with fatal toxicity (gasping syndrome) day (younger than 35 yrs) or 0.0125/kg/
in premature infants. Reconstitute with day (35 yrs and older). CHILDREN: 0.3–
Sterile Water for Injection only. Use 0.7 mg/kg wkly divided into equal daily
only 1 dose per vial. Discard unused doses.
portion. SQ: (Saizen): ADULTS: 0.005 mg/kg/
Reconstitution • Genotropin, Geno­ day. May increase up to 0.01 mg/kg/
tropin Miniquick: Reconstitute with day after 4 wks. CHILDREN: 0.18 mg/
diluent provided. Humatrope: Recon- kg/wk divided into equal daily doses or
stitute with 1.5–5 mL diluent provided, 0.06 mg/kg 3 times/wk or as 0.03 mg/kg
swirl gently, do not shake. Humatrope administered 6 days/wk.
Cartridge: Dilute with solution provided
with cartridge only. Nutropin: Reconsti- Chronic Renal Insufficiency
tute each 5 mg with 1.5–5 mL diluent, swirl SQ: (Nutropin, Nutropin AQ): CHIL-
gently, do not shake. Omnitrope: Recon- DREN: 0.35 mg/kg wkly divided into
stitute with diluents provided, swirl gently, equal daily doses. Continue until the time
do not shake. Saizen: 5 mg: Reconstitute of renal transplantation.
with 1–3 mL diluent provided, swirl gently,
Turner’s Syndrome
do not shake. 8.8 mg: Reconstitute with 2–3
SQ: (Humatrope, Nutropin, Nutro-
mL diluent provided, swirl gently, do not
pin AQ): CHILDREN: 0.375 mg/kg wkly
shake. Serostim: Reconstitute with Sterile
Water for Injection. Zorbtive: Reconsti- divided into equal doses 3–7 times/wk.
(Genotropin, Omnitrope): 0.33 mg/kg
tute with 1–2 mL Bacteriostatic Water for
Injection. wkly divided into 6–7 doses.
Storage • Long-term: Refrigerate all AIDS-Related Wasting
products except Zorbtive. Once recon- SQ: (Serostim): ADULTS WEIGHING
stituted, Humatrope, Nutropin, Saigen, MORE THAN 55 KG: 6 mg once daily at
Zorbtive stable for 14 days, Genotropin bedtime. ADULTS WEIGHING 45–55 KG: 5
for 21 days, Humatrope Cartridge for 28 mg once daily at bedtime. ADULTS WEIGH-
days. Genotropin Miniquick: Refriger- ING 35–44 KG: 4 mg once daily at bedtime.
ate, use within 24 hrs. ADULTS WEIGHING LESS THAN 35 KG: 0.1

INDICATIONS/ROUTES/DOSAGE mg/kg once daily at bedtime.


Growth Hormone Deficiency Short Bowel Syndrome
S SQ: (Genotropin, Omnitrope): SQ: (Zorbtive): ADULTS: 0.1 mg/kg/day.
ADU­LTS: 0.04 mg/kg wkly divided into Maximum: 8 mg/day.
6–7 equal doses/wk. May increase at 4-
to 8-wk intervals to maximum of 0.08 Dosage in Renal/Hepatic Impairment
mg/kg/wk. CHILDREN: 0.16–0.24 mg/kg No dose adjustment.
wkly divided into equal daily doses.
SQ: (Humatrope): ADULTS: 0.006 mg/ SIDE EFFECTS
kg once daily. May increase to maximum Frequent: Otitis media, other ear dis-
of 0.0125 mg/kg/day. CHILDREN: 0.18– orders (with Turner’s syndrome).
0.3 mg/kg wkly divided into alternate-day Occasional: Carpal tunnel syndrome,
doses or 6 doses/wk. gynecomastia, myalgia, peripheral edema,
SQ: (Norditropin): ADULTS: 0.004 mg/ fatigue, asthenia. Rare: Rash, pruritus,
kg/day. May increase after 6 wks up to visual changes, headache, nausea, vomit-
0.016 mg/kg/day. CHILDREN: 0.024– ing, injection site pain/swelling, abdominal
0.034 mg/kg/dose 6–7 days/wk. pain, hip/knee pain.
SQ: (Nutropin, Nutropin AQ):
ADULTS: 0.006 mg/kg once daily. May
increase to maximum of 0.025 mg/kg/

underlined – top prescribed drug


sonidegib 1093
uCLASSIFICATION
ADVERSE EFFECTS/TOXIC
REACTIONS PHARMACOTHERAPEUTIC: Hedge-
Pancreatitis occurs rarely. hog pathway inhibitor. CLINICAL:
Antineoplastic.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT USES
Obtain baseline lab chemistries, thyroid Treatment of adult pts with locally
function, serum glucose level. Obtain full advanced basal cell carcinoma that has
medical history (drug has multiple con- recurred following surgery or radiation
traindications). therapy, or those who are not candidates
for surgery or radiation.
INTERVENTION/EVALUATION
Monitor bone growth, growth rate in PRECAUTIONS
relation to pt’s age. Monitor serum cal- Contraindications: Hypersensitivity to
cium, glucose, phosphorus levels; renal, sonidegib. Cautions: Renal/hepatic impair-
parathyroid, thyroid function. Observe ment. Avoid concomitant use of strong or
for decreased muscle wasting in AIDS pts. moderate CYP3A inhibitors, strong or mod-
PATIENT/FAMILY TEACHING erate CYP3A inducers.
• Follow correct procedure to reconsti- ACTION
tute drug for administration and for safe Basal cell cancer is associated with muta-
handling/disposal of needles. • Regu- tion in Hedgehog pathway components,
lar follow-up with physician is important which can activate the pathway, causing
part of therapy. • Report development nonrestrictive proliferation of skin basal
of severe headache, visual changes, pain cells. Binds to and inhibits smoothened
in hip/knee, limping. homologue (SMO), the protein involved
in Hedgehog signal transduction. Ther-
apeutic Effect: Inhibits tumor cell
sonidegib growth and metastasis.
PHARMACOKINETICS
soe-ni-deg-ib
(Odomzo) Poorly absorbed after PO administration
(less than 10%). Metabolized in liver. S
j BLACK BOX ALERT jMay Protein binding: greater than 97%. Peak
cause embryo-fetal death/severe
malformations when given during plasma concentration: 2–4 hrs. Steady
pregnancy. Verify pregnancy status state reached in 4 mos. Excreted in feces
before initiation. Female patients (70%), urine (30%). Half-life: 28 days.
of reproductive potential must use
effective contraception during LIFESPAN CONSIDERATIONS
treatment and for at least 20 mos
after discontinuation. Due to the Pregnancy/Lactation: May cause fetal
potential risk of exposure through death/malformations. Unknown if distrib-
semen, male patients must use uted in breast milk. Must either discon-
condoms during sexual activity tinue drug or discontinue breastfeeding.
(even after a vasectomy) during
treatment and for at least 8 mos Female patients of reproductive potential
after discontinuation. must use effective contraception during
Do not confuse sonidegib with treatment and up to 20 mos after discon-
vismodegib. tinuation. May compromise female fertility.
Males: Male patients must use condoms
during sexual activity (even after a vasec-
tomy) during treatment and up to 8 mos
Canadian trade name Non-Crushable Drug High Alert drug
1094 sonidegib

after discontinuation. Children: Safety ULN; recurrent severe or intolerable


and efficacy not established. Elderly: May musculoskeletal adverse reactions.
have increased risk of severe musculoskel-
etal adverse events (e.g., muscle spasms, Renal Impairment
myopathy). No dose adjustment.

INTERACTIONS Hepatic Impairment


Mild impairment: No dose adjust-
DRUG: Strong CYP3A inhibitors (e.g.,
clarithromycin, ketoconazole), mod- ment. Moderate to severe impair-
ment: Not studied; use caution.
erate CYP3A inhibitors (e.g., ata-
zanavir, fluconazole) may increase SIDE EFFECTS
concentration/effect. Strong CYP3A
inducers (e.g., carBAMazepine, phe- Frequent (54%–23%): Muscle spasm, alo-
nytoin, rifAMPin) may decrease concen- pecia, dysgeusia, fatigue, nausea, diar-
tration/effect. HERBAL: None significant. rhea, musculoskeletal pain, decreased
FOOD: High-fat meals may increase
appetite. Occasional (19%–10%): Myal-
absorption/concentration. LAB VALUES: gia, abdominal pain, headache, general-
May increase serum ALT/AST, amylase, cre- ized pain, vomiting, pruritus.
atinine, CK, glucose, lipase. May decrease ADVERSE EFFECTS/TOXIC
Hct, Hgb, lymphocytes. REACTIONS
AVAILABILITY (Rx) Musculoskeletal events occurred in 68%
Capsules: 200 mg. of pts. Common Terminology Criteria for
Adverse Events (CTCAE) Grade 3 or 4
ADMINISTRATION/HANDLING musculoskeletal events (9% of pts) may
PO
require administration of muscle relax-
• Give on an empty stomach at least 1 hr ants, analgesics/narcotics, magnesium
before or 2 hrs after a meal. supplementation, IV hydration. Serum CK
level elevations usually occur before mus-
INDICATIONS/ROUTES/DOSAGE culoskeletal pain or spasms. Increased
Basal Cell Carcinoma
serum CK levels reported in 61% of pts.
PO: ADULTS, ELDERLY: 200 mg once The median onset of serum CK elevation
daily. Continue until disease progression was approx. 12 wks. May increase risk
S or unacceptable toxicity. of rhabdomyolysis. Amenorrhea lasting
longer than 18 mos has occurred.
Dose Modification
Interrupt therapy for severe or intoler- NURSING CONSIDERATIONS
able musculoskeletal adverse reactions; BASELINE ASSESSMENT
first occurrence of serum CK level 2.5– Obtain baseline capillary blood glucose,
10 times upper limit of normal (ULN); CBC, LFT, serum CK level, renal function
recurrent serum CK level 2.5–5 times test. Verify negative pregnancy status be-
ULN. Once resolved, resume at 200 mg fore initiation. Question current breast-
once daily. feeding status. Receive medication history
Discontinuation
and screen for interactions. Assess hydra-
Permanently discontinue treatment for tion status. Offer emotional support.
serum CK level greater than 2.5 times ULN INTERVENTION/EVALUATION
with worsening renal function; serum CK Monitor renal function, serum CK levels
level greater than 10 times ULN; recur- periodically and with any musculoskel-
rent serum CK level greater than 5 times etal adverse events. If musculoskeletal
adverse reactions occur with serum CK

underlined – top prescribed drug


SORAfenib 1095
levels greater than 2.5 times ULN, ob- differentiated thyroid carcinoma refractive
tain serum CK level at least wkly until to radioactive iodine treatment. OFF-LABEL:
resolution. Offer antiemetics for nausea/ Recurrent or metastatic angiosarcoma,
vomiting. Monitor urine color, output. resistant gastrointestinal stromal tumor.
Serum CK level elevation or worsening of
renal function may indicate rhabdomy- PRECAUTIONS
olysis. Monitor pregnancy status during Contraindications: Hypersensitivity to
therapy. SORAfenib. Use in combination with
CARBOplatin and PACLitaxel in pts
PATIENT/FAMILY TEACHING
with squamous cell lung cancer. Cau-
• Treatment may cause severe muscle tions: Underlying or poorly controlled
damage, which may cause kidney dam- hypertension, pts with congenital long
age. • Report dark-colored urine or QT syndrome, medications that prolong
decreased urine output despite hydra- QT interval, electrolyte imbalance (hypo-
tion. • Immediately report musculo- kalemia, hypomagnesemia), unstable
skeletal symptoms such as muscle pain/ coronary artery disease, recent MI, HF,
spasms/tenderness/weakness. • Do not concurrent use with strong CYP3A4
donate blood or blood products during inducers.
treatment and up to 20 mos after discon-
tinuation. • Males must use condoms ACTION
during sexual activity during treatment Inhibits tumor cell proliferation by inhib-
and up to 8 mos following discontinua- iting intracellular Raf kinases and cell
tion. • Treatment may cause birth surface kinase receptors. Therapeutic
defects or miscarriage. • Immediately Effect: Inhibits tumor growth and metastasis
report suspected pregnancy. • Hair
loss is an expected side effect. • Swal- PHARMACOKINETICS
low capsules whole; do not chew, crush, Metabolized in liver. Protein binding:
cut or open. • Take on empty stomach 99.5%. Excreted mainly in feces, with
at least 1 hr before or 2 hrs after a meal. lesser amount excreted in urine. Half-
life: 25–48 hrs.
LIFESPAN CONSIDERATIONS
SORAfenib Pregnancy/Lactation: May cause fetal
harm. Adequate contraception should be S
soe-raf-e-nib used during therapy and for at least 2
(NexAVAR) wks after therapy completion. Unknown
Do not confuse NexAVAR with if distributed in breast milk. Breastfeed-
NexIUM, or SORAfenib with ing not recommended. Children: Safety
imatinib or SUNItinib. and efficacy not established. Elderly: No
age-related precautions noted.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Vascular INTERACTIONS
endothelial growth factor (VEGF) DRUG: Strong CYP3A4 inducers (e.g.,
inhibitor. Tyrosine kinase inhibitor. carBAMazepine, PHENobarbital,
CLINICAL: Antineoplastic. rifAMPin) may decrease concentration.
QT interval–prolonging medications
(e.g., amiodarone, azithromycin,
USES
ceritinib, haloperidol, moxifloxacin)
Treatment of advanced renal cell carcinoma, may increase risk of QT interval prolon-
unresectable hepatocellular carcinoma, gation, cardiac arrhythmias. May increase
locally recurrent or metastatic progressive adverse effects of carboplatin. May

Canadian trade name Non-Crushable Drug High Alert drug


1096 SORAfenib
increase anticoagulant effect of warfa- (15%–10%): Constipation, minor bleed-
rin. HERBAL: Echinacea may decrease ing, dyspnea, sensory neuropathy, cough,
the therapeutic effect. St. John’s wort may abdominal pain, dry skin, weight loss, joint
decrease concentration/effect. FOOD: High- pain, headache. Rare (9%–1%): Acne,
fat meals decrease effectiveness. LAB VAL- flushing, stomatitis, mucositis, dyspepsia,
UES: May increase serum lipase, amylase, arthralgia, myalgia, hoarseness.
bilirubin, alkaline phosphatase, transami-
nases. May decrease serum phosphorus, ADVERSE EFFECTS/TOXIC
lymphocytes, WBCs, Hgb, Hct. REACTIONS
Anemia, neutropenia, thrombocytopenia,
AVAILABILITY (Rx) leukopenia occur in less than 10% of pts.
Tablets: (NexAVAR): 200 mg. Pancreatitis, gastritis, erectile dysfunction
occur occasionally. Hemorrhage, cardiac
ADMINISTRATION/HANDLING ischemia/infarction, hypertensive crisis
PO occur rarely.
• Give 1 hr before or 2 hrs after eating
(high-fat meal reduces effective- NURSING CONSIDERATIONS
ness). • Swallow tablet whole; do not BASELINE ASSESSMENT
break, crush, dissolve, or divide tablet. Monitor B/P wkly during first 6 wks of
INDICATIONS/ROUTES/DOSAGE therapy and routinely thereafter. CBC,
serum chemistries including electrolytes,
Renal Cell Carcinoma, Hepatocellular renal function, LFT, chest X-ray should
Carcinoma, Thyroid Carcinoma be performed before therapy begins and
PO: ADULTS, ELDERLY: 400 mg (2 tab- routinely thereafter.
lets) twice daily without food. Continue
until disease progression or unaccept- INTERVENTION/EVALUATION
able toxicity. Determine serum amylase, lipase, phos-
phate concentrations frequently during
Dosage in Renal Impairment therapy. Monitor CBC for evidence of my-
Creatinine elosuppression. Monitor for blood dys-
Clearance Dosage crasias (fever, sore throat, signs of local
40–59 mL/min 400 mg twice daily infection, unusual bruising/bleeding from
20–39 mL/min 200 mg twice daily any site), symptoms of anemia (excessive
S Hemodialysis 200 mg once daily fatigue, weakness). Monitor for signs of
neuropathy (gait disturbances, fine mo-
Dosage in Hepatic Impairment tor control difficulties, numbness).
Bilirubin greater than 1 to 1.5 times
PATIENT/FAMILY TEACHING
upper limit of normal (ULN) and/or
AST greater than ULN: 400 mg twice • Report any episode of chest
daily. Bilirubin greater than 1.5 to 3 pain. • Do not have immunizations
times ULN and any AST: 200 mg twice without physician’s approval (drug low-
daily. Albumin less than 2.5 g/dL (any ers resistance). Avoid contact with those
bilirubin/AST): 200 mg once daily. who have recently taken live virus vac-
cine. • Promptly report fever, sore
SIDE EFFECTS throat, signs of local infection, unusual
Frequent (43%–16%): Diarrhea, rash, bruising/bleeding from any site. • Swal-
fatigue, exfoliative dermatitis, alo- low whole; do not chew, crush, dissolve,
pecia, nausea, pruritus, hyperten- or divide tablet. • Avoid administration
sion, anorexia, vomiting. Occasional after high-fat meals.

underlined – top prescribed drug


sotalol 1097

hypokalemia, hypomagnesemia, renal


sotalol impairment, within first 2 wks post MI,
peripheral vascular disease, Raynaud’s
soe-ta-lol syndrome, myasthenia gravis, psychi-
(Betapace, Betapace AF, Ryosol , atric disease, bronchospastic disease.
Sorine, Sotylize) Concurrent use of digoxin, verapamil,
j BLACK BOX ALERT jInitiation, dilTIAZem, history of severe anaphylaxis
titration to occur in a hospital set- to allergens.
ting with continuous ECG to monitor
potential onset of life-threatening ACTION
arrhythmias. Calculate CrCl prior to
dosing. Adjust dose based on CrCl. Prolongs cardiac action potential, effec-
Betapace should not be substituted tive refractory period, QT interval.
for Betapace AF. Decreases heart rate, AV node conduc-
Do not confuse Betapace with tion; increases AV node refractoriness.
Betapace AF, or sotalol with Therapeutic Effect: Produces antiar-
Stadol or Sudafed. rhythmic activity.
uCLASSIFICATION PHARMACOKINETICS
PHARMACOTHERAPEUTIC: Nonselec- Route Onset Peak Duration
tive beta-adrenergic blocking agent. PO 1–2 hrs 2.5–4 hrs 8–16 hrs
CLINICAL: Antiarrhythmic Class II.
Well absorbed from GI tract. Protein bind-
USES ing: None. Widely distributed. Primarily
excreted unchanged in urine. Removed
Treatment of documented, life-threat- by hemodialysis. Half-life: 12 hrs
ening ventricular arrhythmias. Main- (increased in elderly, renal impairment).
tain normal sinus rhythm in pts with
symptomatic atrial fibrillation/flutter. LIFESPAN CONSIDERATIONS
OFF-LABEL: Fetal tachycardia, treatment
Pregnancy/Lactation: Crosses pla-
of atrial fibrillation with hypertrophic centa. Distributed in breast milk.
cardiomyopathy. Children: Safety and efficacy not estab-
PRECAUTIONS lished. Elderly: Age-related peripheral
Contraindications: Hypersensitivity to vascular disease may increase suscep-
tibility to decreased peripheral circula- S
sotalol. Cardiogenic shock, congenital or
acquired long QT syndrome, second- or tion. Age-related renal impairment may
third-degree heart block (unless func- require dosage adjustment.
tioning pacemaker is present), sinus INTERACTIONS
bradycardia, uncontrolled HF, bronchial
asthma or related bronchospastic condi- DRUG: Calcium channel blockers
tions. Betapace, Betapace AF, Sotyl- (e.g., dilTIAZem, verapamil) may
ize (additional): Baseline QT interval increase effect on AV conduction, B/P.
greater than 450 msec, bronchospastic May mask symptoms of hypoglycemia,
conditions, CrCl less than 40 mL/min, prolong hypoglycemic effects of insu-
serum potassium less than 4 mEq/L, lin, oral hypoglycemics (e.g., glipi-
sick sinus syndrome. Cautions: Pts ZIDE, metFORMIN). QT-prolonging
with history of ventricular tachycardia, medications (e.g., amiodarone,
ventricular fibrillation, cardiomegaly, ciprofloxacin, haloperidol, ondan-
compensated HF, diabetes mellitus, setron) may increase risk of pro-
QT interval prolongation, concurrent longed QT interval. HERBAL: Herbals
medications that prolong QT interval, with hypotensive properties (e.g.,

Canadian trade name Non-Crushable Drug High Alert drug


1098 sotalol

garlic, ginger, ginkgo biloba) may Atrial Fibrillation/Flutter


alter effects. FOOD: None known. LAB Creatinine Clearance Dosage
VALUES: May increase serum BUN, Greater than 60 mL/min 12 hrs
glucose, alkaline phosphatase, LDH, 40–60 mL/min 24 hrs
lipoprotein, ALT, AST, triglycerides, potas- Less than 40 mL/min Contraindicated
sium, uric acid.
Ventricular Arrhythmias
AVAILABILITY (Rx) Creatinine Clearance Dosage
Solution, Intravenous: 150 mg/10 mL. Greater than 60 mL/min 12 hrs
Solution, Oral: 5 mg/mL. Tablets: 80 mg, 30–60 mL/min 24 hrs
120 mg, 160 mg, 240 mg. 10–29 mL/min q36–48h

ADMINISTRATION/HANDLING Dosage in Hepatic Impairment


No dose adjustment.
PO
• Give without regard to food. • Give SIDE EFFECTS
at same time each day. Frequent: Diminished sexual func-
tion, drowsiness, insomnia, asthenia.
INDICATIONS/ROUTES/DOSAGE
Occasional: Depression, cold hands/
Note: Baseline QTc interval and CrCl feet, diarrhea, constipation, anxiety,
must be determined before initiation. nasal congestion, nausea, vomiting.
Ventricular Arrhythmias Rare: Altered taste, dry eyes, pruritus,
PO: ADULTS, ELDERLY: Initially, 80 mg paresthesia of fingers, toes, scalp.
twice daily. May increase in 80-mg incre-
ments at 3-day intervals. Range: 160–320 ADVERSE EFFECTS/TOXIC
mg/day in 2–3 divided doses. Maxi- REACTIONS
mum: 640 mg/day in life-threatening Bradycardia, HF, hypotension, broncho-
refractive arrhythmias. spasm, hypoglycemia, prolonged QT interval,
IV: Initially, 75 mg infused over 5 hrs torsades de pointes, ventricular tachycardia,
twice daily. Range: 75–150 mg twice premature ventricular complexes may occur.
daily. Maximum: 300 mg twice daily.
NURSING CONSIDERATIONS
Atrial Fibrillation, Atrial Flutter
PO: ADULTS, ELDERLY: Initially, 80 mg BASELINE ASSESSMENT
S twice daily. May increase to 120–160 mg Baseline QTc interval and CrCl must be
twice daily. determined prior to initiation. Pt must be
IV: Initially, 75 mg infused over 5 hrs on continuous cardiac monitoring upon
twice daily. Usual dose: 112.5 mg twice initiation of therapy. Do not administer
daily. Maximum: 150 mg twice daily. without consulting physician if pulse is
60 beats/min or less. Question medical
Usual Dosage for Children history as listed in Precautions.
PO: Initially, 90 mg/m2/day
in 3 divided
doses. May incrementally increase up INTERVENTION/EVALUATION
to a maximum of 180 mg/m2/day not to Diligently monitor for arrhythmias. Assess
exceed maximum adult dose of 320 mg/ B/P for hypotension, pulse for bradycardia.
day. Assess for HF: dyspnea, peripheral edema,
jugular vein distention, increased weight,
Dosage in Renal Impairment rales in lungs, decreased urinary output.
Dosage interval is modified based on cre-
PATIENT/FAMILY TEACHING
atinine clearance.
• Do not discontinue, change dose with-
out physician approval. • Avoid tasks
requiring alertness, motor skills until

underlined – top prescribed drug


spironolactone 1099
response to drug is established (may cause declining renal function, ACE inhibitors or
drowsiness). • Periodic lab tests, ECGs angiotensin receptor blockers.
are essential part of therapy. • Report
rapid heartbeat, chest pain, swelling of ACTION
ankles/legs, difficulty breathing. Interferes with sodium reabsorption by
competitively inhibiting action of aldoste-
rone in distal tubule, promoting sodium and
water excretion, increasing potassium reten-
spironolactone tion. May decrease effect of aldosterone on
arteriolar smooth muscle. Therapeutic
spir-on-oh-lak-tone Effect: Produces diuresis, lowers B/P.
(Aldactone, CaroSpir)
j BLACK BOX ALERT j Has PHARMACOKINETICS
been shown to produce tumors in Well absorbed from GI tract (absorption
chronic toxicity animal studies. increased with food). Protein binding:
Do not confuse Aldactone with 91%–98%. Metabolized in liver to active
Aldactazide. metabolite. Primarily excreted in urine.
Unknown if removed by hemodialysis.
FIXED-COMBINATION(S) Half-life: 78–84 min.
Aldactazide: spironolactone/hydro-
CHLOROthiazide (a thiazide diuretic): LIFESPAN CONSIDERATIONS
25 mg/25 mg, 50 mg/50 mg. Pregnancy/Lactation: Active metabo-
lite excreted in breast milk. Breastfeeding
uCLASSIFICATION
not recommended. Children: No age-
PHARMACOTHERAPEUTIC: Aldos- related precautions noted. Elderly: May
terone receptor antagonist. CLINI- be more susceptible to developing hyper-
CAL: Potassium-sparing diuretic, kalemia. Age-related renal impairment
antihypertensive. may require dosage adjustment.
INTERACTIONS
USES
DRUG: ACE inhibitors (e.g., cap-
Management of edema in cirrhotic pts topril, lisinopril), angiotensin
when edema is unresponsive to fluid and receptor blockers (e.g., valsartan),
sodium restriction. Heart failure (NYHA eplerenone, potassium-containing S
class III–IV and reduced ejection frac- medications, potassium supplements
tion) to increase survival, manage edema, may increase risk of hyperkalemia. May
and to reduce need for hospitalization for decrease therapeutic effect of digoxin.
HF. Management of hypertension (unre- NSAIDs (e.g., ibuprofen, ketorolac,
sponsive to other therapies). Treatment naproxen) may decrease antihyper-
of primary hyperaldosteronism. OFF- tensive effect. HERBAL: Herbals with
LABEL: Treatment of edema, hypertension hypertensive properties (e.g., lico-
in children, female acne, female hirsut- rice, yohimbe) or hypotensive prop-
ism. Ascites due to cirrhosis. erties (e.g., garlic, ginger, ginkgo
biloba) may alter effects. FOOD: Food
PRECAUTIONS
increases absorption. LAB VALUES: May
Contraindications: Hypersensitivity to increase urinary calcium excretion,
spironolactone. Hyperkalemia, Addison’s serum BUN, glucose, creatinine, magne-
disease, concomitant use with eplerenone. sium, potassium, uric acid. May decrease
Cautions: Dehydration, hyponatremia, serum sodium.
concurrent use of supplemental potas-
sium, elderly pts, mild renal impairment,

Canadian trade name Non-Crushable Drug High Alert drug


1100 spironolactone

AVAILABILITY (Rx) Dosage in Hepatic Impairment


Oral Suspension: 25 mg/5 mL. No dose adjustment.
Tablets: 25 mg, 50 mg, 100 mg.
SIDE EFFECTS
ADMINISTRATION/HANDLING Frequent: Hyperkalemia (in pts with
PO renal insufficiency, those taking potas-
• Take with food to reduce GI irritation sium supplements), dehydration, hypo-
and increase absorption. Suspension: natremia, lethargy. Occasional: Nausea,
• Shake well. • May give with or with- vomiting, anorexia, abdominal cramps,
out food (give consistently with respect diarrhea, headache, ataxia, drowsiness,
to food). confusion, fever. Male: Gynecomastia,
impotence, decreased libido. Female:
INDICATIONS/ROUTES/DOSAGE Menstrual irregularities (amenorrhea,
Edema (For Cirrhosis) postmenopausal bleeding), breast
PO: ADULTS, ELDERLY: (Tablet): Initially, tender­ness. Rare: Rash, urticaria,
100 mg/day as single dose. May titrate hirsutism.
q3–5 days based on response and tolera-
bility. Maximum dose: 400 mg once daily. ADVERSE EFFECTS/TOXIC
REACTIONS
Hypertension Severe hyperkalemia may produce
PO: ADULTS, ELDERLY: (Tablet): Initially, arrhythmias, bradycardia, ECG changes
12.5–25 mg once daily. May titrate q2wks (tented T waves, widening QRS complex,
as needed. Maximum: 100 mg. (Sus- ST segment depression). May proceed to
pension): 20–100 mg daily in 1 or 2 cardiac standstill, ventricular fibrillation.
divided doses. May titrate q2wks. Cirrhosis pts at risk for hepatic decom-
Primary Aldosteronism pensation if dehydration, hyponatremia
PO: ADULTS, ELDERLY: Initially, 12.5–25 occurs. Pts with primary aldosteronism
mg once daily. Gradually titrate to the may experience rapid weight loss, severe
lowest effective dose. Maximum dose: fatigue during high-dose therapy.
400 mg/day.
NURSING CONSIDERATIONS
HF BASELINE ASSESSMENT
PO: ADULTS, ELDERLY: (Tablet): Initially,
S Weigh pt; initiate strict I&O. Evaluate hy-
12.5–25 mg/day. May double the dose
dration status by assessing mucous mem-
q4wks if serum potassium remains less
branes, skin turgor. Obtain baseline se-
than 5 mEq/L and renal function remains
rum electrolytes, renal/hepatic function,
stable. Maximum: 50 mg/day. in 1 or
urinalysis. Assess for edema; note loca-
2 divided doses. (Suspension): Initially,
tion, extent. Check baseline vital signs,
10–20 mg once daily. May titrate to
note pulse rate/regularity.
37.5 mg once daily if serum potassium
remains less than 5 mEq/L and renal INTERVENTION/EVALUATION
function remains stable. Monitor serum electrolyte values, esp. for
increased potassium, BUN, creatinine.
Dosage in Renal Impairment
Monitor B/P. Monitor for hyponatremia:
CrCl 50 mL/min or greater: Ini-
mental confusion, thirst, cold/clammy
tially, 12.5–25 mg once daily. Main-
skin, drowsiness, dry mouth. Monitor for
tenance: 25 mg once or twice daily.
hyperkalemia: colic, diarrhea, muscle
CrCl 30–49 mL/min: Initially, 12.5 mg
twitching followed by weakness/paraly-
once daily or every other day. Mainte-
sis, arrhythmias. Obtain daily weight.
nance: 12.5–25 mg once daily. CrCl less
Note changes in edema, skin turgor.
than 30 mL/min: Not recommended.

underlined – top prescribed drug


sulfamethoxazole-trimethoprim 1101
PATIENT/FAMILY TEACHING jiroveci pneumonia (PCP), shigellosis,
• Expect increase in volume, frequency enteritis, otitis media, chronic bronchi-
of urination. • Therapeutic effect takes tis, traveler’s diarrhea. Prophylaxis of
several days to begin and can last for PCP. Acute exacerbation of COPD. OFF-
several days when drug is discontinued. LABEL: Chronic prostatitis, prophylaxis
This may not apply if pt is on a potas- for UTI, MRSA infections, prosthetic joint
sium-losing drug concomitantly (diet, infection.
use of supplements should be established
by physician). • Report irregular or PRECAUTIONS
slow pulse, symptoms of electrolyte Contraindications: Hypersensitivity to
imbalance (see previous Intervention/ any sulfa medication, trimethoprim.
Evaluation). • Avoid foods high in History of drug-induced immune
potassium, such as whole grains (cere- thrombocytopenia with sulfonamides
als), legumes, meat, bananas, apricots, or trimethoprim, infants younger than 4
orange juice, potatoes (white, sweet), wks, megaloblastic anemia due to folate
raisins. • Avoid alcohol. • Avoid tasks deficiency, severe hepatic/renal impair-
that require alertness, motor skills until ment. Concomitant administration of
response to drug is established (may dofetilide. Cautions: Pts with G6PD
cause drowsiness). deficiency, impaired renal/hepatic func-
tion, porphyria, pts with allergies or
asthma, elderly pts, alcoholism, thyroid
dysfunction, concurrent anticonvulsant
sulfamethoxazole- therapy.
trimethoprim ACTION
Sulfamethizole: Interferes with bacte-
sul-fa-meth-ox-a-zole-trye-meth- rial folic acid synthesis and growth. Tri-
oh-prim methoprim: Inhibits dihydrofolic acid
(Bactrim, Bactrim DS, Sulfatrim) reduction. Therapeutic Effect: Bacte-
Do not confuse Bactrim with ricidal in susceptible microorganisms.
bacitracin or Bactroban.
PHARMACOKINETICS
FIXED-COMBINATION(S) Rapidly, well absorbed from GI tract.
Bactrim, Septra: sulfamethoxazole/ Protein binding: 45%–60%. Widely dis- S
trimethoprim: 5:1 ratio remains con- tributed. Metabolized in liver. Excreted in
stant in all dosage forms (e.g., 400 urine. Minimally removed by hemodialy-
mg/80 mg). sis. Half-life: sulfamethoxazole, 6–12
hrs; trimethoprim, 6–17 hrs (increased
uCLASSIFICATION
in renal impairment).
PHARMACOTHERAPEUTIC: Sulfona-
mide derivative. CLINICAL: Antibiotic. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Contraindicated
during pregnancy at term and during
USES
lactation. Readily crosses placenta. Dis-
Treatment of susceptible infections due tributed in breast milk. May produce
to S. pneumoniae, H. influenzae, E. kernicterus in newborn. Children: Con-
coli, Klebsiella spp., Enterobacter spp., traindicated in pts younger than 2 mos;
M. morganii, P. mirabilis, P. vulgaris, may increase risk of kernicterus in
S. flexneri, Pneumocystis jiroveci, newborn. Elderly: Increased risk for
including acute or complicated and
recurrent or chronic UTI, Pneumocystis

Canadian trade name Non-Crushable Drug High Alert drug


1102 sulfamethoxazole-trimethoprim
severe skin reaction, myelosuppression, PO
decreased platelet count. • Store tablets, suspension at room tem-
perature. • Administer without regard
INTERACTIONS to food. • Give with at least 8 oz water.
DRUG: May increase concentration/effect
of phenytoin, digoxin, oral hypogly- IV INCOMPATIBILITIES
cemics (e.g., glipiZIDE, metFORMIN), Fluconazole (Diflucan), foscarnet
warfarin. May increase adverse effects of (Foscavir), midazolam (Versed), vinorel-
methotrexate. Strong CYP3A4 induc- bine (Navelbine).
ers (e.g., carBAMazepine, phenytoin,
rifAMPin) may decrease concentration/ IV COMPATIBILITIES
effect. Trimethoprim may increase con- Dexmedetomidine (Precedex), dilTIA-
centration/effect of dofetilide. Leu- Zem (Cardizem), heparin, HYDROmor-
covorin may increase adverse effects of phone (Dilaudid), LORazepam (Ativan),
trimethoprim. HERBAL: St. John’s wort magnesium sulfate, morphine, niCARdip-
may decrease concentration/effect. Herb- ine (Cardene).
als with hypoglycemic properties
(e.g., fenugreek) may increase concen- INDICATIONS/ROUTES/DOSAGE
tration/effect. FOOD: None known. LAB Usual Adult/Elderly Dosage Range
VALUES: May increase serum BUN, cre- PO: 1–2 double-strength tablets
atinine, ALT, AST, bilirubin. q12–24h. IV: 8–20 mg/kg/day as trim-
ethoprim in divided doses q6–12h.
AVAILABILITY (Rx)
b ALERT c All dosage forms have same Usual Dosage Range for Infants 2 Mos and
5:1 ratio of sulfamethoxazole (SMZ) to Older, Children, Adolescents
trimethoprim (TMP). PO/IV: 6–12 mg TMP/kg/day in divided
Injection Solution: SMZ 80 mg and TMP doses q12h. Maximum single dose:
16 mg per mL. Oral Suspension: SMZ 160 mg TMP.
200 mg and TMP 40 mg per 5 mL. Tab- Dosage in Renal Impairment
lets: (Bactrim): SMZ 400 mg and TMP 80
Creatinine
mg. Tablets, Double Strength: (Bactrim DS,
Clearance Dosage
Septra DS): SMZ 800 mg and TMP 160
mg. 15–30 mL/min 50% of usual dosage
Less than 15 Not recommended
S mL/min
ADMINISTRATION/HANDLING
HD 2.5–10 mg/kg trime-
IV thoprim q24h (or 5–20
mg/kg 3 times/wk) (give
Reconstitution • For IV infusion (pig- after HD)
gyback), dilute each 5 mL with 75–125 CRRT 2.5–7.5 mg/kg trime-
mL D5W. • Do not mix with other drugs thoprim q12h
or solutions.
Rate of administration • Infuse over Dosage in Hepatic Impairment
60–90 min. Must avoid bolus or rapid No dose adjustment.
infusion. • Do not give IM. • Ensure
adequate hydration. SIDE EFFECTS
Storage • IV infusion (piggyback) Frequent: Anorexia, nausea, vomiting,
stable for 2 hrs (5 mL/75 mL D5W), 4 hrs rash (generally 7–14 days after therapy
(5 mL/100 mL D5W), 6 hrs (5 mL/125 begins), urticaria. Occasional: Diarrhea,
mL D5W). • Discard if cloudy or pre- abdominal pain, pain/irritation at IV infu-
cipitate forms. sion site. Rare: Headache, vertigo, insom-
nia, seizures, hallucinations, depression.

underlined – top prescribed drug


sulfaSALAzine 1103

ADVERSE EFFECTS/TOXIC Do not confuse Azulfidine with


REACTIONS Augmentin or azaTHIOprine, or
sulfaSALAzine with sulfADIA-
Rash, fever, sore throat, pallor, purpura, ZINE or sulfiSOXAZOLE.
cough, shortness of breath may be early
signs of serious adverse effects. Fatalities uCLASSIFICATION
are rare but have occurred in sulfon- PHARMACOTHERAPEUTIC: 5-Ami-
amide therapy following Stevens-Johnson nosalicylic acid derivative. CLINI-
syndrome, toxic epidermal necrolysis, CAL: Anti-inflammatory.
fulminant hepatic necrosis, agranulocy-
tosis, aplastic anemia, other blood dys-
crasias. Myelosuppression, decreased
platelet count, severe dermatologic reac- USES
tions may occur, esp. in the elderly. Treatment of mild to moderate ulcer-
ative colitis, adjunctive therapy in severe
NURSING CONSIDERATIONS ulcerative colitis, rheumatoid arthritis
BASELINE ASSESSMENT (RA), juvenile rheumatoid arthritis. OFF-
LABEL: Treatment of ankylosing spondy-
Obtain history for hypersensitivity to tri-
methoprim or any sulfonamide, sulfite sen- litis, Crohn’s disease, psoriasis, psoriatic
sitivity, bronchial asthma. Determine serum arthritis.
renal, hepatic, hematologic baselines.
PRECAUTIONS
INTERVENTION/EVALUATION Contraindications: Hypersensitivity to sul-
Monitor daily pattern of bowel activity, stool faSALAzine, sulfa, salicylates; porphyria; GI
consistency. Assess skin for rash, pallor, or GU obstruction. Cautions: Severe aller-
purpura. Check IV site, flow rate. Monitor gies, bronchial asthma, impaired hepatic/
renal, hepatic, hematology function. Assess renal function, G6PD deficiency, blood
I&O. Check for CNS symptoms (headache, dyscrasias, history of recurring or chronic
vertigo, insomnia, hallucinations). Monitor infections.
vital signs at least twice daily. Monitor for
cough, shortness of breath. Assess for overt ACTION
bleeding, ecchymosis, edema. Modulates local mediators of inflam-
matory response. Inhibits tumor ne-
PATIENT/FAMILY TEACHING
crosis factor (TNF). Therapeutic S
• Continue medication for full length of Effect: Decreases inflammatory re-
therapy. • Space doses evenly around sponse, interferes with GI secretion.
the clock. • Take oral doses with 8 oz Effect appears topical rather than sys-
water and drink several extra glasses of temic.
water daily. • Report immediately any
new symptoms, esp. rash, other skin PHARMACOKINETICS
changes, bleeding/bruising, fever, sore Poorly absorbed from GI tract. Cleaved,
throat, diarrhea. • Avoid prolonged absorbed in colon by intestinal bacteria,
exposure to UV, direct sunlight. forming sulfapyridine and mesalamine
(5-ASA). Widely distributed. Metabo-
sulfaSALAzine lized via colonic intestinal flora. Primar-
ily excreted in urine. Half-life: 5.7–10
sul-fa-sal-a-zeen hrs.
(Apo-SulfaSALAzine , Azulfidine,
Azulfidine EN-tabs, Salazopyrin ,
Salazopyrin EN-Tabs )

Canadian trade name Non-Crushable Drug High Alert drug


1104 sulfaSALAzine

LIFESPAN CONSIDERATIONS daily or 1 g/day in 2 divided doses for 1


Pregnancy/Lactation: May produce wk. Increase by 0.5 g/wk, up to 2 g/day in
infertility, oligospermia in men while 2 divided doses. Maximum: 3 g/day (if
taking medication. Readily crosses pla- response to 2 g/day is inadequate after 12
centa; if given near term, may produce wks of treatment).
jaundice, hemolytic anemia, kernicterus
in newborn. Distributed in breast milk. Juvenile Rheumatoid Arthritis (JRA)
Pt should not breastfeed premature PO: (Delayed-Release Tablets): CHIL­
infant or those with hyperbilirubinemia DREN 6–16 YRS: Initially, 10 mg/kg/day.
or G6PD deficiency. Children: No age- May increase by 10 mg/kg/day at wkly
related precautions noted in pts older intervals. Range: 30–50 mg/kg/day.
than 2 yrs. Elderly: No age-related pre- Maximum: 2 g/day.
cautions noted.
Dosage in Renal/Hepatic Impairment
INTERACTIONS Use caution.
DRUG: None significant. HERBAL: None SIDE EFFECTS
significant. FOOD: Impairs folate absorp-
tion. LAB VALUES: None significant. Frequent (33%): Anorexia, nausea, vomit-
ing, headache, oligospermia (generally
AVAILABILITY (Rx) reversed by withdrawal of drug). Occa-
sional (3%): Hypersensitivity reaction
Tablets: (Azulfidine): 500 mg.
(rash, urticaria, pruritus, fever, anemia).
Tablets, Delayed-Release: (Azulfidine Rare (less than 1%): Tinnitus, hypoglyce-
EN-tabs): 500 mg. mia, diuresis, photosensitivity.
ADMINISTRATION/HANDLING ADVERSE EFFECTS/TOXIC
PO REACTIONS
• Space doses evenly (intervals not to Anaphylaxis, Stevens-Johnson syndrome,
exceed 8 hrs). • Administer after meals hematologic toxicity (leukopenia, agran-
or with food. • Swallow enteric-coated ulocytosis), hepatotoxicity, nephrotoxic-
tablets whole; do not break, crush, dis- ity occur rarely.
solve, or divide. • Give with 8 oz of
water; encourage several glasses of water NURSING CONSIDERATIONS
S between meals.
BASELINE ASSESSMENT
INDICATIONS/ROUTES/DOSAGE Question for hypersensitivity to medica-
Ulcerative Colitis tions. Check initial urinalysis, CBC, serum
PO: ADULTS, ELDERLY: Initially, 3-4 g/ renal function, LFT.
day in divided doses q8h. May initiate INTERVENTION/EVALUATION
at 1-2 g/day to reduce GI intolerance.
Maximum: 6 g/day. Maintenance: 2 Monitor I&O, urinalysis, renal function
g/day in divided doses at intervals less tests; ensure adequate hydration (mini-
than or equal to q8h. CHILDREN 6 YRS AND mum output 1,500 mL/24 hrs) to prevent
OLDER: Initially, 40–70 mg/kg/day in 3–6 nephrotoxicity. Assess skin for rash (dis-
divided doses. Maximum initial dose: continue drug, notify physician at first
4 g/day. Maintenance: 30–70 mg/kg/ sign). Monitor daily pattern of bowel ac-
day in 3–6 divided doses. Maximum tivity, stool consistency. (Dosage increase
daily dose: 4 g/day. may be needed if diarrhea continues,
recurs.) Monitor CBC closely; assess for
Rheumatoid Arthritis (RA) and report immediately any hematologic
PO: (Delayed-Release Tablets): effects (bleeding, ecchymoses, fever,
ADU­LTS, ELDERLY: Initially, 0.5 g once
underlined – top prescribed drug
SUMAtriptan 1105
pharyngitis, pallor, weakness, purpura). or basilar migraine, peripheral vascu-
Monitor LFT; observe for jaundice. lar disease, CVA, ischemic heart disease
(including angina pectoris, history of MI,
PATIENT/FAMILY TEACHING
silent ischemia, Prinzmetal’s angina),
• May cause orange-yellow discolor- severe hepatic impairment, transient
ation of urine, skin. • Space doses ischemic attack, uncontrolled hyperten-
evenly around the clock. • Take after or sion, MAOI use within 14 days, use within
with food with 8 oz of water; drink several 24 hrs of ergotamine preparations or
glasses of water between meals. • Swal- another 5-HT1 agonist. Cautions: Mild
low enteric-coated tablets whole; do not to moderate hepatic impairment, history
chew, crush, dissolve, or divide tab- of seizure disorder, controlled hyperten-
lets. • Continue for full length of treat- sion, elderly pts.
ment; may be necessary to take drug even
after symptoms relieved. • Routinely ACTION
monitor blood levels. • Inform dentist, Binds selectively to serotonin 5-HT1
surgeon of sulfaSALAzine ther- receptors in cranial arteries, producing
apy. • Avoid exposure to sun, ultraviolet vasoconstrictive effect on cranial blood
light until photosensitivity determined vessels. Therapeutic Effect: Relieves
(may last for mos after last dose). migraine headache.
PHARMACOKINETICS
Route Onset Peak Duration
SUMAtriptan Nasal 15 min N/A 24–48 hrs
PO 30 min 2 hrs 24–48 hrs
soo-ma-trip-tan SQ 10 min 1 hr 24–48 hrs
(Imitrex, Onzetra, Sumavel DosePro,
Xsail, Zembrace SymTouch) Rapidly absorbed after SQ administra-
Do not confuse SUMAtriptan tion. Absorption after PO administra-
with SAXagliptin, SITagliptin, tion is incomplete; significant amounts
somatropin, or ZOLMitriptan. undergo hepatic metabolism, resulting
in low bioavailability (about 14%). Pro-
FIXED-COMBINATION(S) tein binding: 10%–21%. Widely distrib-
Treximet: SUMAtriptan/naproxen (an uted. Undergoes first-pass metabolism
NSAID): 85 mg/500 mg, 10 mg/60 mg. in liver. Excreted in urine. Half-life: S
2 hrs.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Serotonin LIFESPAN CONSIDERATIONS
5-HT1 receptor agonist. CLINICAL: An- Pregnancy/Lactation: Unknown if dis-
timigraine. tributed in breast milk. Children: Safety
and efficacy not established. Elderly: No
age-related precautions noted.
USES
PO, SQ, Intranasal, Transdermal: INTERACTIONS
Acute treatment of migraine headache DRUG: Ergotamine-containing medi-
with or without aura. SQ: (Exclud- cations may produce vasospastic
ing Zembrace) Treatment of cluster reaction. MAOIs (e.g., phenelzine,
headaches. selegiline) may increase concentration,
half-life. SSRIs (e.g., escitalopram,
PRECAUTIONS PARoxetine, sertraline) and SNRIs
Hypersensitivity to
Contraindications: (e.g., DULoxetine, venlafaxine) may
SUMAtriptan. Management of hemiplegic increase risk of serotonin syndrome.

Canadian trade name Non-Crushable Drug High Alert drug


1106 SUMAtriptan
HERBAL: None significant. FOOD: None SQ: ADULTS, ELDERLY: Initially, up to 6
known. LAB VALUES: None significant. mg. Maximum: Up to two 6-mg injec-
AVAILABILITY (Rx) tions/24 hrs (separated by at least 1 hr).
(Zembrace SymTouch): 3-mg single
Injection, Prefilled Autoinjector: 4 dose. Maximum: 12 mg/24 hrs. Sepa-
mg/0.5 mL, 6 mg/0.5 mL. (Zembrace rate dose by at least 1 hr.
SymTouch): 3-mg prefilled syringe. Intranasal: ADULTS, ELDERLY: (Spray):
Injection Solution: (Imitrex): 4 mg/0.5 Initially, 5 mg, 10 mg, or 20 mg once in
mL, 6 mg/0.5 mL. (Sumavel DosePro): 4 one nostril. May repeat once after at least
mg/0.5 mL, 6 mg/0.5 mL. Nasal Powder: 2 hrs. Maximum: 40 mg/24h. (Nasal
(Onzetra, Xsail): Capsules: 11 mg (to be Powder): Initially, a single dose of 22 mg
used with Xsail breath powdered nasal (11 mg in each nostril). May repeat once
device). Nasal Spray: (Imitrex Nasal): 5 after at least 2hrs. Maximum: 44 mg/24
mg/actuation, 20 mg/actuation. Tablets: hrs separated by at least 2 hrs.
(Imitrex): 25 mg, 50 mg, 100 mg.
Cluster Headaches
ADMINISTRATION/HANDLING SQ: ADULTS, ELDERLY: Initially, 6 mg.
SQ May repeat after 1 hr. Maximum: 6 mg/
• Follow manufacturer’s instructions for dose; two 6-mg doses/24 hrs.
autoinjection device use. • Administer
needleless (Sumavel DosePro) only to Dosage in Renal Impairment
abdomen or thigh. No dose adjustment.
PO Dosage in Hepatic Impairment
• Swallow tablets whole. Do not break, Mild to moderate impairment:
crush, dissolve, or divide. • Take with Maximum PO dose: 50 mg. Severe
full glass of water. impairment: Contraindicated.

Nasal SIDE EFFECTS


• Unit contains only one spray—do not Frequent: PO (10%–5%): Tingling, nasal
test before use. • Instruct pt to gently discomfort. SQ (greater than 10%): Injec-
blow nose to clear nasal pas- tion site reactions, tingling, warm/hot sen-
sages. • With head upright, close one sation, dizziness, vertigo. Nasal (greater
S nostril with index finger, breathe out than 10%): Altered taste, nausea, vomit-
gently through mouth. • Have pt insert ing. Occasional: PO (5%–1%): Flushing,
nozzle into open nostril about one-half asthenia, visual disturbances. SQ (10%–
inch, close mouth and, while taking a 2%): Burning sensation, numbness, chest
breath through nose, release spray dos- discomfort, drowsiness, asthenia. Nasal
age by firmly pressing plunger. • Instruct (5%–1%): Nasopharyngeal discomfort,
pt to remove nozzle from nose and gently dizziness. Rare: PO (less than 1%): Agita-
breathe in through nose and out through tion, eye irritation, dysuria. SQ (less than
mouth for 10–20 sec; do not breathe in 2%): Anxiety, fatigue, diaphoresis, muscle
deeply. cramps, myalgia. Nasal (less than 1%):
Burning sensation.
INDICATIONS/ROUTES/DOSAGE
ADVERSE EFFECTS/TOXIC
Acute Migraine Headache
REACTIONS
PO: ADULTS, ELDERLY: 50–100 mg. Dose
may be repeated after at least 2 hrs. Excessive dosage may produce tremors,
Maximum: 100 mg/single dose; 200 redness of extremities, reduced respira-
mg/24 hrs. tions, cyanosis, seizures, paralysis. Serious
arrhythmias occur rarely, esp. in pts with

underlined – top prescribed drug


SUNItinib 1107

hypertension, obesity, smokers, diabetes, USES


strong family history of coronary artery Treatment of GI stromal tumor (GIST)
disease. Serotonin syndrome may occur after disease progression while on or
(agitation, confusion, hallucinations, hyper- demonstrating intolerance to imatinib.
reflexia, myoclonus, shivering, tachycardia). Treatment of advanced renal cell carci-
noma (RCC). Adjuvant treatment of adults
NURSING CONSIDERATIONS at high risk of recurrent RCC following
BASELINE ASSESSMENT nephrectomy. Treatment of pancreatic
Receive full medical history, medication neuroendocrine tumor (PNET). OFF-
history and screen for contraindications. LABEL: Non-GI stromal tumor, soft tissue
Obtain pregnancy test in female pts of sarcomas, advanced thyroid cancer.
reproductive potential. Question regard-
PRECAUTIONS
ing onset, location, duration of migraine,
possible precipitating symptoms. Contraindications: Hypersensitivity to
SUNItinib. Cautions: Cardiac dysfunction,
INTERVENTION/EVALUATION bradycardia, electrolyte imbalance, bleed-
Evaluate for relief of migraine headache ing tendencies, hypertension, history of
and resulting photophobia, phonophobia prolonged QT interval, medications that
(sound sensitivity), nausea, vomiting. prolong QT interval, hypokalemia, hypo-
magnesemia, concurrent use of strong
PATIENT/FAMILY TEACHING CYP3A4 inducers or inhibitors, HF, renal/
• Follow proper technique for loading of hepatic impairment, pregnancy.
autoinjector, injection technique, discard-
ing of syringe. • Do not use more than 2 ACTION
injections during any 24-hr period and Inhibitory action against multiple receptor
allow at least 1 hr between injec- tyrosine kinases including growth factor
tions. • Report immediately if wheezing, receptors, vascular endothelial growth
palpitations, skin rash, facial swelling, factors, colony-stimulating factor recep-
pain/tightness in chest/throat occur. tors, glial cell-line neurotrophic factor
receptors. Therapeutic Effect: Pre-
vents tumor cell growth, produces tumor
regression, inhibits metastasis.
SUNItinib PHARMACOKINETICS S
soo-nit-in-ib Metabolized in liver. Protein binding:
(Sutent) 95%. Excreted in feces (61%), urine
j BLACK BOX ALERT jHepato- (16%). Half-life: 40–60 hrs.
toxicity may be severe and/or result
in fatal liver failure. LIFESPAN CONSIDERATIONS
Do not confuse SUNItinib with Pregnancy/Lactation: Has potential for
imatinib or SORAfenib. embryotoxic, teratogenic effects. Breastfeed-
ing not recommended. Children: Safety
uCLASSIFICATION and efficacy not established. Elderly: No
PHARMACOTHERAPEUTIC: Vascular age-related precautions noted.
endothelial growth factor (VEGF)
inhibitor. Tyrosine kinase inhibitor. INTERACTIONS
CLINICAL: Antineoplastic. DRUG: Strong CYP3A4 inhibitors (e.g.,
clarithromycin, itraconazole, keto-
conazole, voriconazole) may increase
concentration, toxicity. Strong CYP3A4
inducers (e.g., carBAMazepine,
Canadian trade name Non-Crushable Drug High Alert drug
1108 SUNItinib

PHENobarbital, phenytoin, rifAMPin) Concomitant Use of CYP3A4 Inducers


may decrease concentration/effects. QT Consider a dose increase (monitor care-
interval–prolonging medications (e.g., fully for toxicity) to maximum of 87.5
amiodarone, haloperidol, moxifloxa- mg/day (GIST, RCC) or 62.5 mg (PNET).
cin) may increase risk of QT interval prolon-
gation, cardiac arrhythmias. May increase Dosage in Renal Impairment
adverse effects of bevacizumab. May No initial dose adjustment; subsequent
increase adverse effects; decrease therapeu- adjustment may be needed.
tic effect of vaccines (live). HERBAL: St. Dosage in Hepatic Impairment
John’s wort may decrease concentration. No dose adjustment initially; Grade 3 or
Herbals with hypoglycemic properties 4 hepatotoxicity during treatment: with-
(e.g., fenugreek) may increase hypoglyce- hold/discontinue if hepatotoxicity does
mic effect. Echinacea may decrease thera- not resolve.
peutic effect. FOOD: Grapefruit products
may increase concentration/effect. LAB SIDE EFFECTS
VALUES: May increase serum alkaline Stromal tumor: Common (42%–30%):
phosphatase, bilirubin, amylase, lipase, cre- Fatigue, diarrhea, anorexia, abdominal
atinine, ALT, AST. May alter serum potassium, pain, nausea, hyperpigmentation. Fre-
sodium, uric acid. May produce thrombocy- quent (29%–18%): Mucositis/stomatitis,
topenia, neutropenia. May decrease serum vomiting, asthenia, altered taste, constipa-
phosphate, thyroid function levels. tion, fever. Occasional (15%–8%): Hyper-
AVAILABILITY (Rx) tension, rash, myalgia, headache,
arthralgia, back pain, dyspnea, cough.
Capsules: 12.5 mg, 25 mg, 37.5 mg, Renal carcinoma: Common (74%–43%):
50 mg. Fatigue, diarrhea, nausea, mucositis/sto-
ADMINISTRATION/HANDLING matitis, dyspepsia, altered taste. Frequent
(38%–20%): Rash, vomiting, constipation,
PO
hyperpigmentation, anorexia, arthralgia,
• Give without regard to food. Avoid dyspnea, hypertension, headache, abdom-
grapefruit products. inal pain. Occasional (18%–11%): Limb
INDICATIONS/ROUTES/DOSAGE pain, peripheral/periorbital edema, dry
GI Stromal Tumor, Renal Cell Carcinoma,
skin, hair color change, myalgia, cough,
S RCC (Adjuvant Treatment)
back pain, dizziness, fever, tongue pain,
PO: ADULTS, ELDERLY: 50 mg once daily for
flatulence, alopecia, dehydration.
4 wks, followed by 2 wks off in 6-wk cycle. ADVERSE EFFECTS/TOXIC
REACTIONS
Pancreatic Neuroendocrine Tumor
PO: ADULTS, ELDERLY: 37.5 mg once Palmar-plantar erythrodysesthesia syn-
daily continuously without a scheduled off- drome (PPES) occurs occasionally
treatment period. Maximum: 50 mg/day. (14%), manifested as blistering/rash/
peeling of skin on palms of hands, soles
Dose Modification of feet. Bleeding, decrease in left ventric-
PO: ADULTS, ELDERLY: Dosage increase or ular ejection fraction, deep vein throm-
reduction in 12.5-mg increments is recom- bosis (DVT), pancreatitis, neutropenia,
mended based on safety and tolerability. seizures occur rarely.
Concomitant Use of Strong CYP3A4 NURSING CONSIDERATIONS
Inhibitors
BASELINE ASSESSMENT
Consider a dose reduction to a minimum
of 37.5 mg/day (GIST, RCC) or 25 mg/ Question possibility of pregnancy. Obtain
day (PNET). baseline CBC, BMP, LFT before beginning

underlined – top prescribed drug


suvorexant 1109
therapy and prior to each treatment. Obtain ACTION
baseline ECG, thyroid function tests. Ques- Suppresses wake drive of the orexin neu-
tion medical history as listed in Precautions. ropeptide signaling system, the central pro-
INTERVENTION/EVALUATION moter of wakefulness. Blocks binding of
Assess eye area, lower extremities for orexin neuropeptides orexin A and orexin B
early evidence of fluid retention. Offer to receptors of OX1R and OX2R. Therapeu-
antiemetics to control nausea, vomiting. tic Effect: Induces sleep with fewer night-
Monitor daily pattern of bowel activity, time awakenings; improves sleep pattern.
stool consistency. Monitor CBC for evi- PHARMACOKINETICS
dence of neutropenia, thrombocytopenia;
assess LFT for hepatotoxicity. Monitor for Rapidly absorbed. Metabolized in liver.
PPES. Monitor B/P. Protein binding: greater than 99%. Peak
plasma concentration: 2 hrs. Excreted
PATIENT/FAMILY TEACHING in feces (66%), urine (23%). Half-
• Avoid crowds, those with known infec- life: 12 hrs.
tion. • Avoid contact with anyone who
recently received live virus vaccine. • Do LIFESPAN CONSIDERATIONS
not have immunizations without physi- Pregnancy/Lactation: Unknown if dis-
cian’s approval (drug lowers resis- tributed in breast milk. Children: Safety
tance). • Avoid pregnancy; use effective and efficacy not established. Elderly: No
contraceptive measures. • Promptly age-related precautions noted.
report fever, unusual bruising/bleeding
from any site. INTERACTIONS
DRUG: Alcohol, CNS depressants
(e.g., LORazepam, morphine, zol-
suvorexant pidem) may increase CNS depression.
Moderate CYP3A4 inhibitors (e.g.,
ciprofloxacin, dilTIAZem), strong
soo-voe-rex-ant
CYP3A4 inhibitors (e.g., clarithromy-
(Belsomra)
cin, ketoconazole) may increase con-
uCLASSIFICATION centration/effect, CNS depression. Strong
CYP3A4 inducers (e.g., rifAMPin,
PHARMACOTHERAPEUTIC: Orexin re-
phenytoin) may decrease concentra-
ceptor antagonist. CLINICAL: Hypnotic. S
tion/effect. May increase concentration/
effect of digoxin. HERBAL: Herbals with
USES sedative properties (e.g., chamomile,
Treatment of insomnia, characterized by kava kava, valerian) may increase CNS
difficulties with sleep onset and/or sleep depression. St. John’s wort may decrease
maintenance. concentration/effect. FOOD: Grapefruit
products may increase concentration/
PRECAUTIONS effect. LAB VALUES: May increase serum
Contraindications: Hypersensitivity to cholesterol.
suvo­ rexant. History of narcolepsy. Cau-
tions: History of COPD, depression, debil-
AVAILABILITY (Rx)
itation, drug dependency, obstructive sleep Tablets: 5 mg, 10 mg, 15 mg, 20 mg.
apnea, respiratory disease, pts at high risk
of suicide; concomitant use of CNS depres- ADMINISTRATION/HANDLING
sants, strong CYP3A4 inhibitors/inducers. PO
Concomitant use of other insomnia medi- • Administer no more than once per night,
cations not recommended. within 30 min of bedtime. • Do not admin-
ister unless 7 hrs or greater is dedicated for
Canadian trade name Non-Crushable Drug High Alert drug
1110 suvorexant
sleep. • For faster sleep onset, do not give while “asleep” have been reported.
with or immediately after meal. May increase risk of suicidal ideation,
worsening of depression. Sleep paraly-
INDICATIONS/ROUTES/DOSAGE sis (inability to move or speak for up
Insomnia to several min during sleep-wake tran-
PO: ADULTS, ELDERLY: 10 mg once daily sitions) and hypnagogic/hypnopompic
within 30 min of bedtime. May increase hallucinations (including vivid and dis-
to 20 mg. turbing perceptions) may occur.
Dose Modification NURSING CONSIDERATIONS
Concomitant use with other CNS
depressants, moderate CYP3A4 BASELINE ASSESSMENT
inhibitors: Decrease starting dose to 5 Assess sleep pattern, ability to fall asleep.
mg once at bedtime. May increase to 10 Provide environment conductive to rest-
mg once at bedtime. Concomitant use ful sleep. Initiate fall precautions. Raise
of strong CYP3A4 inhibitors: Not bed rails, provide call light. Receive full
recommended. Daytime somno- medication history, including herbal
lence: Decrease dose or discontinue if products, and screen for medication
daytime somnolence. interactions. Question history of comor-
bidities, esp. mental health disorders,
Dosage in Renal Impairment substance abuse.
No dose adjustment.
INTERVENTION/EVALUATION
Dosage in Hepatic Impairment Monitor sleep pattern. Evaluate for thera-
Mild to moderate impairment: No peutic response: decrease in number of
dose adjustment. Severe impair- nocturnal awakenings, increase in length
ment: Not recommended. of sleep. Diligently monitor for daytime
somnolence and CNS depressant effects
SIDE EFFECTS regardless of compliance. Worsening of
Occasional (7%): Headache, somno- insomnia, emergence of new cognitive or
lence. Rare (3%–2%): Dizziness, diar- behavioral abnormalities, or treatment
rhea, dry mouth, upper respiratory tract failure after 7–10 days may indicate un-
infection, abnormal dreams, cough. derlying psychiatric disorder.
S ADVERSE EFFECTS/TOXIC PATIENT/FAMILY TEACHING
REACTIONS • Report nighttime episodes of “sleep”
Obese pts and female pts may have driving, preparing food, making phone
increased exposure-related effects com- calls, or having sex while not fully
pared to nonobese pts and male pts, awake. • Do not abruptly discontinue
respectively. May impair daytime wake- medication after long-term use. • Avoid
fulness even when taken as prescribed. tasks that require alertness, motor skills
Impairment can occur in the absence until drug response estab-
of symptoms and may not be reliably lished. • Treatment may cause next-day
detected by ordinary clinical exam. CNS impairment, drowsiness, or falling asleep
depression may persist for up to several while driving despite taking medication
days. May increase risk of falling asleep as prescribed (esp. pts taking higher
while driving. Abnormal thinking and doses). • Do not ingest alcohol or
behavioral changes such as amnesia, grapefruit products. • Do not take drug
anxiety, lowered sexual inhibition, hal- unless a full night can be dedicated to
lucinations, and driving, preparing and sleep. • Immediately report worsening
eating meals, and making phone calls of depression or thoughts of suicide.

underlined – top prescribed drug


tacrolimus 1111
other nephrotoxic drugs (e.g., cycloSPO-
tacrolimus RINE), concurrent use of strong CYP3A4
inhibitors or inducers. Avoid use of po-
ta-kroe-li-mus tassium-sparing diuretics, ACE inhibitors,
(Astagraf XL, Envarsus XR, Prograf, potassium-based salt substitutes. Pts at
Protopic) risk for pure red cell aplasia (e.g., concur-
j BLACK BOX ALERT jIncreased rent use of mycophenolate); pts at risk for
susceptibility to infection and QT prolongation, hypokalemia, hypomag-
potential for development of nesemia. Topical: Exposure to sunlight.
lymphoma. Extended-release as-
sociated with increased mortality in ACTION
female liver transplant recipients.
Topical form associated with rare Inhibits T-lymphocyte activation by binding
cases of malignancy. Topical form to intracellular protein FKBP-12, forming a
should be used only for short-term complex with calcineurin-dependent pro-
and intermittent treatment. Use in
children younger than 2 yrs of age teins, inhibiting calcineurin phosphatase
not recommended. Use only 0.03% activity. Therapeutic Effect: Suppresses
ointment for children 2–15 yrs of immunologically mediated inflammatory re-
age. Administer under supervision sponse; prevents organ transplant rejection.
of physician experienced in im-
munosuppressive therapy. PHARMACOKINETICS
Do not confuse Protopic with Variably absorbed after PO administra-
Protonix, or tacrolimus with tion (food reduces absorption). Protein
everolimus, pimecrolimus, binding: 99%. Metabolized in liver. Pri-
sirolimus, or temsirolimus. marily excreted in feces. Not removed by
uCLASSIFICATION hemodialysis. Half-life: 21–61 hrs.
PHARMACOTHERAPEUTIC: Cal- LIFESPAN CONSIDERATIONS
cineurin inhibitor. CLINICAL: Immu-
nosuppressant. Pregnancy/Lactation: Crosses pla-
centa. Hyperkalemia, renal dysfunction
noted in neonates. Distributed in breast
USES milk. Breastfeeding not recommended.
PO, Injection: Prevention of organ re- Children: May require higher dosages
jection in pts receiving allogeneic liver, (decreased bioavailability, increased clear-
kidney, heart transplant. Should be used ance). May make post-transplant lympho-
concurrently with adrenal corticoste- proliferative disorder more common, esp.
roids. In heart and kidney transplant pts, in pts younger than 3 yrs. Elderly: Age- T
should be used in conjunction with aza- related renal impairment may require dos-
THIOprine or mycophenolate. Topical: age adjustment.
Moderate to severe atopic dermatitis in
immunocompetent pts. OFF-LABEL: Pre- INTERACTIONS
vention of organ rejection in lung, small DRUG: Aluminium-containing antac-
bowel recipients; prevention and treat- ids may increase concentration. Strong
ment of graft-vs-host disease in allogeneic CYP3A4 inhibitors (e.g., clarithromy-
hematopoietic stem cell transplantation. cin, ketoconazole, ritonavir), calcium
channel blockers (e.g., dilTIAZem,
PRECAUTIONS verapamil) may increase concentra-
Contraindications: Hypersensitivity to tion/effects. Strong CYP3A4 inducers
tacrolimus. Cautions: Hypersensitivity to (e.g., carBAMazepine, phenytoin,
HCO-60 polyoxyl 60 hydrogenated castor rifAMPin) may decrease concentration/
oil (used in solution for injection). Renal/ effects. CycloSPORINE, foscarnet may
hepatic impairment, concurrent use with increase nephrotoxic effect. May decrease
Canadian trade name Non-Crushable Drug High Alert drug
1112 tacrolimus
therapeutic effect; increase a­ dverse effect of 2 hrs after a meal. Do not crush, cut,
vaccines (live). Enzalutamide may de- dissolve, or divide; swallow whole.
crease concentration/effect. Eplerenone,
potassium-sparing diuretics (e.g., spi- Topical
ronolactone) may increase hyperkalemic • For external use only. • Do not
effect. HERBAL: Echinacea may decrease cover with occlusive dressing. • Rub
therapeutic effect. St. John’s wort may gently, completely onto clean, dry skin.
decrease concentration/effect. FOOD: Food
decreases rate/extent of absorption. Grape- IV INCOMPATIBILITIES
fruit products may increase concentration, Acyclovir.
toxicity (potential for nephrotoxicity). LAB
VALUES: May increase serum ALT, AST,
IV COMPATIBILITIES
amylase, bilirubin, BUN, cholesterol, creati- Calcium gluconate, dexamethasone
nine, potassium, glucose, triglycerides. May (Decadron), diphenhydrAMINE (Bena-
decrease serum magnesium; Hgb, Hct, plate- dryl), DOBUTamine (Dobutrex), DOPa-
lets. May alter leukocytes. mine (Intropin), furosemide (Lasix), hepa-
rin, HYDROmorphone (Dilaudid), insulin,
AVAILABILITY (Rx) leucovorin, LORazepam (Ativan), mor-
Capsules: (Prograf): 0.5 mg, 1 mg, 5 mg. phine, nitroglycerin, potassium chloride.
Injection Solution: (Prograf): 5 mg/mL.
INDICATIONS/ROUTES/DOSAGE
Ointment: (Protopic): 0.03%, 0.1%.
Note: Give initial postoperative dose no
Capsules, Extended-Release: ­(Astagraf
sooner than 6 hrs after liver or heart trans-
XL): 0.5 mg, 1 mg, 5 mg. Tablets, Extended-
plant and within 24 hrs of kidney transplant.
Release: (Envarsus XR): 0.75 mg, 1 mg, 4
mg. Prevention of Liver Transplant Rejection
PO: ADULTS, ELDERLY: (Immediate-Re-
ADMINISTRATION/HANDLING lease): 0.1–0.15 mg/kg/day in 2 divided
IV doses 12 hrs apart (in combination with
corticosteroids). Titrate to target trough
Reconstitution • Dilute with appro- concentration. CHILDREN: 0.15–0.2 mg/
priate amount (250–1,000 mL, depend- kg/day in 2 divided doses 12 hrs apart.
ing on desired dose) 0.9% NaCl or D5W Titrate to target trough concentration.
to provide concentration between 0.004 IV: ADULTS, ELDERLY, CHILDREN: 0.03–
and 0.02 mg/mL. 0.05 mg/kg/day as continuous infusion.
Rate of administration • Give as con-
T tinuous IV infusion. • Continuously moni- Prevention of Kidney Transplant Rejection
tor pt for anaphylaxis for at least 30 min after PO: ADULTS, ELDERLY: (Immediate-
start of infusion. • Stop infusion immedi- Release): 0.2 mg/kg/day (in combination
ately at first sign of hypersensitivity reaction. with azaTHIOprine) in 2 divided doses 12
Storage • Store diluted infusion solu- hrs apart or 0.1 mg/kg/day (in combina-
tion in glass or polyethylene containers tion with mycophenolate) in 2 divided
and discard after 24 hrs. • Do not store doses 12 hrs apart. Titrate to target trough
in PVC container (decreased stability, concentration. (Extended-Release
potential for extraction). [Astagraf XL]): (With Basiliximab In-
duction): (Prior to or within 48 hrs of
PO transplant completion): 0.15–0.2 mg/kg
• Avoid grapefruit products. • Im- once daily (in combination with corticoste-
mediate-Release: Administer without roids and mycophenolate). Titrate to target
regard to food. Be consistent with timing trough concentration. (Without Basilix-
of administration. • Extended-Re- imab Induction): Preoperative dose: 0.1
lease: Administer at least 1 hr before or mg/kg (administer within 12 hrs prior to
underlined – top prescribed drug
talazoparib 1113
reperfusion). Postoperative dosing: 0.2 ication history and screen for interaction
mg/kg once daily (in combination with (esp. use of other immunosuppressants).
corticosteroids and mycophenolate). Give Have aqueous solution of EPINEPHrine
at least 4 hrs after preoperative dose and 1:1,000, O2 available at bedside before
within 12 hrs of reperfusion. Titrate to tar- beginning IV infusion.
get trough concentration. (Extended-Re-
INTERVENTION/EVALUATION
lease [Envarsus XL]): 0.14 mg/kg/day.
IV: ADULTS, ELDERLY: 0.03–0.05 mg/kg/ CBC should be performed wkly during
day as continuous infusion. first mo of therapy, twice monthly during
second and third mos of treatment, then
Prevention of Heart Transplant Rejection monthly throughout the first yr. Monitor
Note: Recommended in combination BUN, serum creatinine, CrCL, eGFR pts
with azaTHIOprine or mycophenolate. with renal impairment. Monitor LFT pe-
PO: ADULTS, ELDERLY: Initially, 0.075 mg/ riodically. Assess continuously for first 30
kg/day in 2 divided doses 12 hrs apart. Ti- min following start of infusion and at fre-
trate to target trough concentration. quent intervals thereafter. Monitor I&O
IV: ADULTS, ELDERLY: 0.01 mg/kg/day as closely. Monitor for infections.
continuous infusion.
PATIENT/FAMILY TEACHING
Atopic Dermatitis • Treatment may depress your immune
Topical: ADULTS, ELDERLY, CHILDREN 15 system and reduce your ability to fight in-
YRS AND OLDER: Apply 0.03% or 0.1% fection. Report symptoms of infection
ointment to affected area twice daily. CHIL- such as body aches, burning with urina-
DREN 2–15 YRS: Use 0.03% ointment. Con- tion, chills, cough, fatigue, fever. Avoid
tinue treatment for 1 wk after symptoms those with active infection. • Report de-
have resolved. If no improvement within creased urination, chest pain, headache,
6 wks, re-examine to confirm diagnosis. dizziness, respiratory infection, rash, un-
usual bleeding/bruising. • Avoid expo-
SIDE EFFECTS sure to sun, artificial light (may cause
Frequent (greater than 30%): Headache, photosensitivity reaction). • Do not take
tremor, insomnia, paresthesia, diarrhea, within 2 hrs of taking antacids. • Do
nausea, constipation, vomiting, ab- not ingest grapefruit products.
dominal pain, hypertension. Occasional
(29%–10%): Rash, pruritus, anorexia,
asthenia, peripheral edema, photosen-
sitivity. talazoparib T
ADVERSE EFFECTS/TOXIC tal-a-zoe-pa-rib
REACTIONS (Talzenna)
Nephrotoxicity (elevated serum cre- Do not confuse talazoparib with
atinine, decreased urinary output), neu- niraparib, olaparib, or ruca-
rotoxicity (tremor, headache, altered parib, or Talzenna with Senna.
mental status), pleural effusion occur uCLASSIFICATION
commonly. Thrombocytopenia, leukocy-
tosis, anemia, atelectasis, sepsis, infec- PHARMACOTHERAPEUTIC: Poly (ADP-
tion occur occasionally. ribose) polymerase (PARP) inhibi-
tor. CLINICAL: Antineoplastic.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT USES
Screen for active infection. Question his- Treatment of adults with deleterious or
tory of renal impairment. Receive full med- suspected deleterious germline BRCA-
Canadian trade name Non-Crushable Drug High Alert drug
1114 talazoparib
mutation (gBRCAm) HER2-negative lo- INTERACTIONS
cally advanced or metastatic breast cancer. DRUG: Certain P-gp inhibitors (e.g.,
amiodarone, carvedilol, clarithro-
PRECAUTIONS
mycin, itraconazole, verapamil) may
Contraindications: Hypersensitivity to significantly increase concentration/
talazoparib. Cautions: Baseline anemia, effect. Cladribine may increase myelo-
leukopenia, neutropenia, thrombocyto- suppression. HERBAL: None significant.
penia; renal/hepatic impairment, con- FOOD: None known. LAB VALUES: May in-
ditions predisposing to infection (e.g., crease serum alkaline phosphatase, ALT,
diabetes, renal failure, immunocompro- AST, glucose. May decrease Hgb, leuko-
mised pts, open wounds); concomitant cytes, neutrophils, lymphocytes, platelets;
use of P-gp inhibitors. Do not initiate in serum calcium.
pts who have not recovered from hema-
tological toxicities related to prior che- AVAILABILITY (Rx)
motherapy. Capsules: 0.25 mg, 1 mg.
ACTION
ADMINISTRATION/HANDLING
Inhibits poly (ADP-ribose) polymerase
PO
(PARP) enzymatic activity. PARP enzymes
• Give without regard to meals. • Adminis-
are involved in DNA transcription, cell
ter capsules whole; do not break, cut, or
cycle regulation and DNA repair. Inhibi-
open. Capsules cannot be chewed. • If a
tion causes cell death due to DNA dam-
dose is missed or vomiting occurs after
age. Therapeutic Effect: Inhibits tumor
administration, do not give extra dose. Ad-
cell growth and metastasis.
minister next dose at regularly scheduled
PHARMACOKINETICS time.
Widely distributed. Metabolized by oxi- INDICATIONS/ROUTES/DOSAGE
dation, dehydrogenation, and conjuga- Note: Administer only to pts with germ-
tion (with minimal hepatic metabolism). line BRCA mutation.
Protein binding: 74%. Peak plasma con-
centration: 1–2 hrs. Excreted in urine Breast Cancer
(69%), feces (20%). Half-life: 90 PO: ADULTS, ELDERLY: 1 mg once daily.
(±58) hrs. Continue until disease progression or
unacceptable toxicity.
LIFESPAN CONSIDERATIONS
T Pregnancy/Lactation: Avoid preg- Dose Reduction Schedule
nancy; may cause fetal harm. Female First reduction: 0.75 mg once daily.
pts of reproductive potential must use Second reduction: 0.5 mg once daily.
effective contraception during treatment Third reduction: 0.25 mg once daily.
and for at least 7 mos after discontinu- Unable to tolerate 0.25 mg dose:
ation. Unknown if distributed in breast Permanently discontinue.
milk. Breastfeeding not recommended
during treatment and for at least 1 mo Dose Modification
after discontinuation. Males: Male pts Based on Common Terminology Criteria
with female partners of reproductive for Adverse Events (CTCAE).
potential must use effective contracep- Hematologic Toxicity
tion during treatment and for at least 4 Hemoglobin less than 8 g/dL: With-
mos after discontinuation. May impair hold treatment until improved to 9 g/
fertility. Children: Safety and efficacy not dL (or greater), then resume at next re-
established. Elderly: No age-related pre- duced dose.
cautions noted.
underlined – top prescribed drug
talazoparib 1115
Platelet count less than 50,000 cells/
NURSING CONSIDERATIONS
mm3: Withhold treatment until improved
to 75,000 cells/mm3 (or greater), then BASELINE ASSESSMENT
resume at next reduced dose. Neutro- Obtain CBC; pregnancy test in female pts
phil count less than 1,000 cells/ of reproductive potential. Question plans
mm3: Withhold treatment until im- of breastfeeding. Confirm compliance
proved to 1,500 cells/mm3 (or greater), of effective contraception. Obtain renal
then resume at next reduced dose. function test (BUN, serum creatinine,
CrCl, eGFR) in pts with renal impairment;
Nonhematologic Toxicity
LFTs in pts with hepatic impairment.
Any Grade 3 or 4 adverse reaction:
Question history of hepatic/renal impair-
Withhold treatment until improved to ment, prior treatment with other chemo-
Grade 1 or 0, then consider resuming at therapeutic agents. Receive full medica-
a reduced dose or discontinue. tion history and screen for interactions
Concomitant Use of P-gp Inhibitors (esp. P-gp inhibitors). Screen for active
Reduce dose to 0.75 mg once daily. If infection. Do not initiate in pts who have
P-gp inhibitor is discontinued for 3–5 not recovered from hematological toxici-
half-lives, resume talazoparib dose to ties related to prior chemotherapy. Offer
the dose used prior to starting P-gp in- emotional support.
hibitor. INTERVENTION/EVALUATION
Dosage in Renal Impairment Monitor CBC monthly. If hematologic
Mild impairment: No dose adjustment. toxicities occur, monitor CBC wkly until
Moderate impairment (CrCl 30–59 blood counts recover. If blood counts do
mL/min): Reduce dose to 0.75 mg once not recover, consider hematology consul-
daily. Severe impairment: Not speci- tation for further investigations such as
fied; use caution. bone marrow analysis and blood sample
for cytogenetics. Monitor for acute my-
Dosage in Hepatic Impairment eloid leukemia, myelodysplastic syn-
Mild impairment: No dose adjustment. drome (bleeding, bruising easily; fatigue,
Moderate to severe impairment: Not frequent infections, pyrexia, hematuria,
specified; use caution. melena, weakness, weight loss; cytope-
nias, increased requirements for blood
SIDE EFFECTS transfusion). If acute myeloid leukemia
Frequent (62%–21%): Fatigue, asthenia, or myelodysplastic syndrome occurs, dis-
nausea, headache, vomiting, alopecia, continue treatment. If concomitant use of T
diarrhea, decreased appetite. P-gp inhibitor is unavoidable, monitor
for adverse reactions/drug toxicities.
ADVERSE EFFECTS/TOXIC Diligently screen for infections. Monitor
REACTIONS daily pattern of bowel activity, stool con-
Myelosuppression (anemia, leukopenia, sistency. Encourage nutritional intake.
neutropenia, thrombocytopenia) has PATIENT/FAMILY TEACHING
occurred. Grade 3 (or higher) anemia,
neutropenia, thrombocytopenia reported • Treatment may depress your immune
in 39%–15% of pts. Acute myeloid leu- system and reduce your ability to fight
kemia, myelodysplastic syndrome was infection. Report symptoms of infection
reported in pts who received prior che- such as body aches, burning with urina-
motherapy with platinum agents and/or tion, chills, cough, fatigue, fever. Avoid
DNA-damaging agents. those with active infection. • Treatment
may cause severe bone marrow depres-
sion or new-onset myeloid leukemia;

Canadian trade name Non-Crushable Drug High Alert drug


1116 tamoxifen
r­eport bruising, fatigue, fever, frequent OFF-LABEL: Ovarian cancer (advanced and/
infections, shortness of breath, weight or recurrent), treatment of endometrial
loss; bleeding easily, blood in urine or cancer; risk reduction of breast cancer in
stool. • Avoid pregnancy. Female pts of women with Paget’s disease of the breast.
childbearing potential must use effective
contraception during treatment and for PRECAUTIONS
at least 7 mos after last dose. Do not Contraindications:Hypersensitivity to
breastfeed. Male pts with female partners tamoxifen. Concomitant warfarin therapy
of childbearing potential must use effec- when used in treatment of breast cancer
tive contraception during treatment and in high-risk women, history of deep vein
for at least 4 mos after last dose. • Treat- thrombosis (DVT) or pulmonary embolism
ment may impair fertility in males. • Re- (in high-risk women for breast cancer and
port liver problems (abdominal pain, in women with DCIS). Cautions: Throm-
bruising, clay-colored stool, amber- or bocytopenia, pregnancy, history of throm-
dark-colored urine, yellowing of the skin boembolic events, hyperlipidemia, con-
or eyes). • There is a high risk of inter- comitant strong CYP2D6 inhibitors and/or
actions with other medications. Do not moderate CYP2D6 inhibitors.
take newly prescribed medications un-
less approved by prescriber who origi- ACTION
nally started treatment. Competitively binds to estrogen receptors
on tumor, producing a complex. Thera-
peutic Effect: Inhibits DNA synthesis and
estrogen effects. Slows tumor growth.
tamoxifen
PHARMACOKINETICS
ta-MOKS-i-fen Well absorbed from GI tract. Metabolized
(Nolvadex-D , Soltamox) in liver. Primarily excreted in feces. Half-
j BLACK BOX ALERT jSerious, life: 7 days.
possibly life-threatening CVA, pul-
monary emboli, uterine malignancy LIFESPAN CONSIDERATIONS
(endometrial adenocarcinoma, Pregnancy/Lactation: If possible,
uterine sarcoma) have occurred. avoid use during pregnancy, esp. first tri-
Do not confuse tamoxifen with mester. May cause fetal harm. Unknown if
pentoxifylline, tamsulosin, or distributed in breast milk. Breastfeeding
temazepam. not recommended. Nonhormonal con-
T traceptives recommended during therapy
uCLASSIFICATION and for at least 2 mos after discontinu-
PHARMACOTHERAPEUTIC: Selec- ation. Children: Safe and effective in
tive estrogen receptor modulator girls 2–10 yrs with McCune-Albright syn-
(SERM). Estrogen receptor antago- drome, precocious puberty. Elderly: No
nist. CLINICAL: Antineoplastic. age-related precautions noted.
INTERACTIONS
USES DRUG: Strong CYP3A4 inducers (e.g.,
Adjunct treatment in advanced breast can- carBAMazepine, phenytoin, rifAMPin)
cer after primary treatment with surgery may decrease concentration/effect. Strong
and radiation, reduction of risk of breast CYP3A4 inhibitors (e.g., clarithromy-
cancer in women at high risk, reduction cin, ketoconazole) may increase concen-
of risk of invasive breast cancer in women tration/effect. May i­ncrease effect of warfa-
with ductal carcinoma in situ (DCIS), meta- rin. May decrease effect of anastrozole.
static breast cancer in women and men. Moderate/strong CYP2D6 inhibitors

underlined – top prescribed drug


tamoxifen 1117
(e.g., FLUoxetine, sertraline) may de- SIDE EFFECTS
crease efficacy and increase risk of breast Frequent: Women (greater than 10%):
cancer. HERBAL: St. John’s wort may de- Hot flashes, nausea, vomiting. Occa-
crease concentration/effects. FOOD: None sional: Headache, nausea, vomiting, rash,
known. LAB VALUES: May increase serum bone pain, confusion, weakness, drowsi-
cholesterol, calcium, triglycerides, AST, ALT. ness. Women (9%–1%): Changes in
menstruation, genital itching, vaginal dis-
AVAILABILITY (Rx) charge, endometrial hyperplasia, p­ olyps.
Solution, Oral: (Soltamox): 10 mg/5 mL. Men: Impotence, decreased libido.
Tablets: 10 mg, 20 mg.
ADVERSE EFFECTS/TOXIC
ADMINISTRATION/HANDLING REACTIONS
PO Retinopathy, corneal opacity, decreased
• Give without regard to food. • Use visual acuity noted in pts receiving ex-
supplied dosing cup for oral solution. tremely high dosages (240–320 mg/day)
for longer than 17 mos.
INDICATIONS/ROUTES/DOSAGE
Metastatic Breast Cancer (Males and NURSING CONSIDERATIONS
Females) BASELINE ASSESSMENT
PO: ADULTS, ELDERLY: 20–40 mg/day.
Obtain CBC, serum calcium, estrogen
Give doses greater than 20 mg/day in 2 receptor assay prior to therapy. Obtain
divided doses. baseline breast and gynecologic exams,
Breast Cancer Treatment mammogram results. Question history of
PO: ADJUVANT THERAPY (FEMALES), PRE- thrombosis (DVT, PE).
MENOPAUSAL WOMEN: 20 mg once daily INTERVENTION/EVALUATION
for 5 yrs. May continue for total of 10 yrs if Obtain CBC, serum calcium periodically.
premenopausal or perimenopausal after 5 Be alert to increased bone pain; en-
yrs. If postmenopausal after 5 yrs, may con- sure adequate pain relief. Monitor I&O,
tinue for total of 10 yrs or switch to an AI up weight. Monitor for symptoms of DVT
to total of 10 yrs of endocrine therapy. POST- (leg or arm pain/swelling), PE (chest
MENOPAUSAL WOMEN: Total duration of 10
pain, dyspnea, tachycardia). Assess for
yrs, or tamoxifen for an initial duration of 5 hypercalcemia (increased urinary vol-
yrs, followed by an AI for up to 5 yrs (for to- ume, excessive thirst, nausea, vomiting,
tal duration of 10 yrs) or tamoxifen for 2–3 constipation, hypotonicity of muscles,
yrs, followed by an AI for up to 5 yrs (for a T
deep bone/flank pain, renal stones).
total duration of 7–8 yrs) or an AI for 5 yrs.
PATIENT/FAMILY TEACHING
Ductal Carcinoma in Situ (DCIS)
• Report vaginal bleeding/discharge/itch-
PO: ADULTS, ELDERLY: 20 mg once daily ing, leg cramps, weight gain, shortness of
for 5 yrs. breath, weakness. • May initially experi-
Breast Cancer Risk Reduction ence increase in bone, tumor pain (appears
PO: ADULTS, ELDERLY: 20 mg once daily to indicate good tumor response). • Re-
for 5 yrs. port persistent nausea, vomiting. • Report
symptoms of DVT (e.g., swelling, pain, hot
Dosage in Renal/Hepatic Impairment feeling in the arms or legs; discoloration of
No dose adjustment. extremity), lung embolism (e.g., difficulty
breathing, chest pain, rapid heart
rate). • Nonhormonal contraceptives are
recommended during treatment.

Canadian trade name Non-Crushable Drug High Alert drug


1118 tamsulosin

LIFESPAN CONSIDERATIONS
tamsulosin Pregnancy/Lactation: Not indicated
tam-soo-loe-sin for use in women. Children: Not indi-
(Flomax, Flomax CR ) cated in this pt population. Elderly: No
Do not confuse Flomax with age-related precautions noted.
­Flonase, Flovent, Foltx, INTERACTIONS
­Fosamax, or Volmax, or
­tamsulosin with tamoxifen DRUG: Other alpha-adrenergic block-
or terazosin. ing agents (e.g., doxazosin, prazosin,
terazosin) may increase alpha-blockade
FIXED-COMBINATION(S) effects. Sildenafil, tadalafil, vardenafil
Jalyn: tamsulosin/dutasteride (an may cause symptomatic hypotension.
androgen hormone inhibitor): 0.4 Strong CYP3A4 inhibitors (e.g., clar-
mg/0.5 mg. ithromycin, ketoconazole, ritona-
vir) may increase concentration. Strong
uCLASSIFICATION CYP3A4 inducers (e.g., carBAMaze-
PHARMACOTHERAPEUTIC: Alpha 1- pine, phenytoin, rifAMPin) may decrease
adrenergic blocker. CLINICAL: Be- concentration/effect. HERBAL: Herbals
nign prostatic hyperplasia agent. with hypotensive properties (e.g.,
garlic, ginger, ginkgo biloba) may al-
ter effects. St. John’s wort may decrease
concentration/effect. FOOD: Grapefruit
USES products may increase risk for orthostatic
hypotension. LAB VALUES: None known.
Treatment of symptoms of benign pros-
tatic hyperplasia (BPH). OFF-LABEL: AVAILABILITY (Rx)
Treatment of bladder outlet obstruction
or dysfunction. To facilitate expulsion of Capsules: 0.4 mg.
ureteral stones (distal).
ADMINISTRATION/HANDLING
PRECAUTIONS PO
Contraindications: Hypersensitivity to • Give at same time each day, 30 min
tamsulosin. Cautions: Concurrent use after the same meal. • Do not break,
of phosphodiesterase (PDE5) inhibitors crush, or open capsule.
(e.g., sildenafil, tadalafil, vardenafil), pts
INDICATIONS/ROUTES/DOSAGE
T with orthostatic hypotension.
Benign Prostatic Hyperplasia (BPH)
ACTION PO: ADULTS: 0.4 mg once daily, ap-
Antagonist of alpha receptors in prostate. proximately 30 min after same meal each
Therapeutic Effect: Relaxes smooth day. May increase dosage to 0.8 mg if in-
muscle in bladder neck and prostate; im- adequate response in 2–4 wks.
proves urinary flow, symptoms of pros-
Dosage in Renal/Hepatic Impairment
tatic hyperplasia.
No dose adjustment.
PHARMACOKINETICS SIDE EFFECTS
Well absorbed, widely distributed.
Frequent (9%–7%): Dizziness, drowsiness.
Protein binding: 94%–99%. Metabo-
­
Occasional (5%–3%): Headache, anxiety,
lized in liver. Primarily excreted in urine.
insomnia, orthostatic hypotension. Rare
­Unknown if removed by hemodialysis.
(less than 2%): Nasal congestion, pharyn-
Half-life: 9–13 hrs.
gitis, rhinitis, nausea, vertigo, impotence.

underlined – top prescribed drug


tapentadol 1119

ADVERSE EFFECTS/TOXIC uCLASSIFICATION


REACTIONS PHARMACOTHERAPEUTIC: Centrally
First-dose syncope (hypotension with acting opioid (Schedule II). CLINI-
sudden loss of consciousness) may oc- CAL: Analgesic.
cur within 30–90 min after initial dose.
May be preceded by tachycardia (pulse
rate of 120–160 beats/min). USES
Nucynta: Relief of moderate to severe
NURSING CONSIDERATIONS acute pain in adults 18 yrs and older. Nu-
BASELINE ASSESSMENT
cynta ER: Management of moderate to
severe chronic or neuropathic pain asso-
Assess history of prostatic hyperplasia ciated with diabetic peripheral neuropa-
(difficulty initiating urine stream, drib- thy when around-the-clock analgesic is
bling, sense of urgency, leaking). Ques- needed for extended period.
tion for sensitivity to tamsulosin, or use of
other alpha-adrenergic blocking agents.
PRECAUTIONS
Obtain vital signs.
Contraindications: Hypersensitivity to ta-
INTERVENTION/EVALUATION pentadol. Severe respiratory depression,
Assist with ambulation if dizziness oc- acute or severe bronchial asthma, hyper-
curs. Monitor renal function, I&O, weight capnia in uncontrolled settings, known or
changes, peripheral edema, B/P. Monitor suspected paralytic ileus, concurrent use or
for first-dose syncope. ingestion within 14 days of MAOI use. Cau-
tions: Respiratory disease or respiratory
PATIENT/FAMILY TEACHING compromise (e.g., hypoxia, hypercapnia,
• Take at same time each day, 30 min or decreased respiratory reserve), asthma,
after the same meal. • Go from lying to COPD, severe obesity, sleep apnea syn-
standing slowly. • Avoid tasks that re- drome, CNS depression, pts with head in-
quire alertness, motor skills until re- jury, intracranial lesions, pancreatic or bili-
sponse to drug is established. • Do not ary disease, renal or hepatic impairment,
break, crush, open capsule. • Avoid seizure disorder, conditions that increase
grapefruit products. risk of seizures, pts at risk for hypotension,
adrenal insufficiency, concurrent use with
serotonergic agents, elderly pts, debilitated
or cachetic pts. History of substance abuse.
tapentadol T
ACTION
ta-pen-ta-dol Binds to mu-opioid receptors in the cen-
(Nucynta, Nucynta ER, Nucynta IR ) tral nervous system, causing inhibition
j BLACK BOX ALERT j of ascending pain pathways; increases
Exposes pt to risks of opioid addic-
tion, abuse, misuse. Serious, life- norepinephrine by inhibiting its reab-
­
threatening respiratory depression sorption into nerve cells. Therapeutic
may occur. Accidental ingestion Effect: Produces analgesia. Reduces
can result in a fatal overdose. May level of pain perception.
cause neonatal opioid withdrawal
syndrome. Avoid alcohol while PHARMACOKINETICS
taking tapentadol ER. Benzodi-
azepines, CNS depressants may Metabolized in liver. Primarily excreted
cause profound sedation, respira- in the urine. Widely distributed. Protein
tory depression, coma, or death. binding: 20%. Half-life: 4 hrs.
Do not confuse tapentadol with
traMADol.

Canadian trade name Non-Crushable Drug High Alert drug


1120 tapentadol

LIFESPAN CONSIDERATIONS Release Tapentadol): Use same total


Pregnancy/Lactation: Unknown if daily dose but divide into 2 equal doses given
drug crosses placenta or is distributed twice daily. Maximum: 500 mg daily.
in breast milk. Children: Not recom- Neuropathic Pain Associated with
mended for use in this pt population. Diabetic Peripheral Neuropathy
Elderly: Age-related renal impairment PO: ADULTS, ELDERLY: (Extended-­
may increase risk of side effects. Release): Initially, 50 mg q12h. Titrate
INTERACTIONS in increments of 50 mg no more fre-
quently than twice daily q3days. Range:
DRUG: Alcohol, CNS depressants 100–250 mg q12h.
(e.g., LORazepam, morphine, zol-
pidem) may increase CNS depres- Dosage in Renal Impairment
sion, respiratory depression. MAOIs CrCl 30 mL/min or greater: No
(e.g., phenelzine, selegiline), adjustment. CrCl less than 30 mL/
SSRIs (e.g., FLUoxetine) may in- min: Not recommended.
crease risk of serotonin syndrome.
HERBAL: Herbals with sedative Dosage in Hepatic Impairment
properties (e.g., chamomile, kava (Immediate-Release): Moderate im-
kava, valerian) may increase CNS pairment: 50 mg q8h. Maximum: 3
depression. FOOD: None known. LAB doses/24 hrs. (Extended-Release): Ini-
VALUES: None significant. tially, 50 mg/day. Maximum: 100 mg/day.
AVAILABILITY (Rx) SIDE EFFECTS
Tablets: 50 mg, 75 mg, 100 mg. Frequent (greater than 10%): Nausea, diz-
50 mg,
Tablets, Extended-Release:
ziness, vomiting, sleepiness, headache.
100 mg, 150 mg, 200 mg, 250 mg. ADVERSE EFFECTS/TOXIC
REACTIONS
ADMINISTRATION/HANDLING
Respiratory depression, serotonin syn-
PO
drome have been reported.
• Give without regard to food. • Tab-
lets may be crushed. • Give extended-
release tablets whole; do not break, NURSING CONSIDERATIONS
crush, dissolve, or divide.
BASELINE ASSESSMENT
INDICATIONS/ROUTES/DOSAGE Assess onset, type, location, and duration
T of pain. Obtain vital signs before giving
Note: Not recommended in severe renal
or hepatic impairment. medication. If respirations are 12/min or
lower, withhold medication, contact phy-
Pain Control sician. Question medical history as listed
PO: ADULTS, ELDERLY: (Nucynta): 50–100 in Precautions.
mg q4–6h as needed (may administer an ad-
INTERVENTION/EVALUATION
ditional dose 1h or longer after initial dose).
Maximum: 600 mg/day (700 mg on day 1). Be alert for decreased respirations or B/P.
(Nucynta ER): Initially, 50 mg twice daily Initiate deep breathing and coughing ex-
(12 hrs apart). May increase by 50 mg twice ercises, particularly in pts with impaired
daily q3days to effective dose. Range: 100– pulmonary function. Assess for clinical im-
250 mg twice daily. Maximum: 500 mg/day. provement and record onset of pain relief.
PATIENT/FAMILY TEACHING
Conversion to Extended-Release
Conversion from other oral opi- • Avoid tasks that require alertness, mo-
oids: Initially, 50 mg q12h. (Immediate- tor skills until response to drug is estab-

underlined – top prescribed drug


tedizolid 1121
lished. • Avoid alcohol, CNS depres- LIFESPAN CONSIDERATIONS
sants. • Report nausea, vomiting, Pregnancy/Lactation: Unknown
shortness of breath, difficulty breathing. if distributed in breast milk. Chil-
dren: Safety and efficacy not established
in pts younger than 18 yrs. Elderly: No
tedizolid age-related precautions noted.
INTERACTIONS
ted-eye-zoe-lid
(Sivextro) DRUG: May decrease effect of BCG (in-
Do not confuse tedizolid with travesical). Maprotiline, buprenor-
linezolid. phine, tapentadol, carBAMazepine
may enhance adverse/toxic effects.
uCLASSIFICATION May enhance hypertensive effect of bu-
PHARMACOTHERAPEUTIC: Oxazo- PROPion. HERBAL: None significant.
lidinone-class antibacterial. CLINI- FOOD: None known. LAB VALUES: May
CAL: Antibiotic. decrease Hgb, platelets, neutrophils. May
increase serum ALT, AST.

USES AVAILABILITY (Rx)


Treatment of adult pts with acute bacte- Lyophilized Powder for Injection: 200
rial skin and skin structure infections mg/vial. Tablets: 200 mg.
(ABSSSI) caused by susceptible strains ADMINISTRATION/HANDLING
of gram-positive microorganisms includ-
ing Staphylococcus aureus (including IV
methicillin-susceptible and methicillin-
resistant strains), S. agalactiae, S. an- • Vials contain no preservatives or bac-
ginosus group (including S. anginosus, teriostatic agents. • Must reconstitute
S. intermedius, S. constellatus), S. pyo- with Sterile Water for Injection and sub-
genes, and E. faecalis. sequently dilute with 0.9% NaCl
only. • Do not inject as IV push or
PRECAUTIONS ­bolus.
Reconstitution • Reconstitute vial
Contraindications: Hypersensitivity to te-
dizolid. Cautions: History of C. difficile with 4 mL of Sterile Water for Injec-
infection or antibiotic-associated colitis, tion. • To avoid foaming, alternate be-
myelosuppression, neutropenia, periph- tween gentle swirling and inversion until
powder is completely dissolved. If foam- T
eral/optic neuropathy.
ing occurs, let vial stand until foam
ACTION ­dispersed. • Visually inspect for
Inhibits cellular protein synthesis by ­particulate matter or discoloration. Do
binding to 50S subunit of bacterial ribo- not use if particulate matter is ob-
some. Therapeutic Effect: Antibiotic served. • Withdraw 4 mL of solution
(bacteriostatic). with vial in upright position; do not invert
vial during draw-up. • Further dilute in
PHARMACOKINETICS 250 mL 0.9% NaCl. • Gently invert bag
Readily absorbed following PO adminis- to mix; do not shake.
Rate of administration • Infuse over
tration. Protein binding: 70%–90%. Peak
plasma concentration: PO: 3 hrs; IV: end 1 hr via dedicated line.
Storage • Reconstituted solution should
of infusion. Excreted in feces (82%),
urine (18%). Minimally removed by he- appear clear, colorless to yellow. • Admin-
modialysis. Half-life: 12 hrs. ister within 24 hrs of reconstitution. • May

Canadian trade name Non-Crushable Drug High Alert drug


1122 teduglutide
refrigerate or store solution at room tem- NURSING CONSIDERATIONS
perature up to 24 hrs.
BASELINE ASSESSMENT
PO Obtain baseline CBC (note WBC, bands),
• Give without regard to food. wound culture/sensitivity, vital signs.
IV INCOMPATIBILITIES Question history of recent C. difficile in-
fection, hypersensitivity reaction. Assess
Any solutions containing divalent cations skin wound characteristics; hydration
(e.g., Ca2+, Mg2+), lactated Ringer’s injec- status. Question pt’s usual stool charac-
tion. Do not infuse with other medications. teristics (color, frequency, consistency).
INDICATIONS/ROUTES/DOSAGE INTERVENTION/EVALUATION
Acute Bacterial Skin and Skin Structure Monitor skin infection/wound for im-
Infection provement. Monitor daily pattern of
PO, IV: ADULTS, ELDERLY: 200 mg once bowel activity, stool consistency; increas-
daily for 6 days. ing severity may indicate antibiotic-as-
sociated colitis. If frequent diarrhea oc-
Dosage in Renal/Hepatic Impairment curs, obtain C. difficile toxin screen and
No dose adjustment. initiate isolation precautions until result
SIDE EFFECTS confirmed. Encourage PO intake. Moni-
tor I&O. Monitor for infusion-related/
Occasional (8%–3%): Nausea, headache, hypersensitivity reaction.
diarrhea, vomiting. Rare (2%): Dizziness,
dermatitis, insomnia. PATIENT/FAMILY TEACHING
• It is essential to complete drug therapy
ADVERSE EFFECTS/TOXIC despite symptom improvement. Early dis-
REACTIONS continuation may result in antibacterial
Safety and efficacy in pts with neutrope- resistance or an increased risk of recur-
nia not established. Antibacterial activity rent infection. • Report episodes of di-
may be reduced in the absence of granu- arrhea, esp. following wks after treatment
locytes. C. difficile–associated diarrhea completion. Frequent abdominal pain,
with severity ranging from mild diarrhea blood-streaked stool, diarrhea, fever, may
to fatal colitis has been reported for up indicate infectious diarrhea, which may
to 2 mos following administration. Treat- be contagious. • Drink plenty of fluids.
ment in the absence of proven or strongly
T suspected bacterial infection may in-
crease risk of drug-resistant bacteria. teduglutide
Infusion/hypersensitivity reactions (pru-
ritus, urticaria, flushing, hypertension, te-due-gloo-tide
palpitations, tachycardia), optic disor- (Gattex, Revestive )
ders (asthenopia, blurry vision, neuropa- Do not confuse teduglutide
thy, visual impairment, vitreous floaters), with liraglutide or albiglutide,
neurologic disorders (hypoesthesia, par- or Gattex with Gas-X.
esthesia, peripheral neuropathy, cranial
nerve VII paralysis), infections (oral can- uCLASSIFICATION
didiasis, vulvovaginal mycotic infection) PHARMACOTHERAPEUTIC: Gluca-
occur rarely. gon-like peptide-2 (GLP-2) analogue.
CLINICAL: Short bowel syndrome
(short gut syndrome, short gut) agent.

underlined – top prescribed drug


teduglutide 1123

USES has a white snap-off cap, snap or twist off


Treatment of adults and pediatric pts 1 yr white cap. • If diluent syringe has a
and older with short bowel syndrome (SBS) gray screw top, unscrew top counter-
who are dependent on parenteral support. clockwise. • Push prefilled syringe into
vial containing teduglutide. • After all
PRECAUTIONS diluent has gone into vial, remove sy-
Contraindications: Hypersensitivity to tedu- ringe, needle and discard. • Allow vial
glutide. Cautions: Cardiovascular disease, to sit for 30 sec. • Gently roll vial for 15
HF, pts at increased risk for malignancy, bil- sec (do not shake) and let stand for 2
iary tract (gallbladder, pancreatic) disease, min. • Withdraw prescribed dose, dis-
hypervolemia, stenosis, renal impairment. card remaining fluid.
Administration • Insert needle sub-
ACTION cutaneously into upper arms, outer thigh,
Analogue of naturally occurring peptide or abdomen, and inject solution. • Do
secreted in distal intestine, known to in- not inject into areas of active skin disease
crease intestinal, portal blood flow, and or injury such as sunburns, skin rashes,
inhibit gastric secretion. Therapeutic inflammation, skin infections, or active
Effect: Improves intestinal absorption. psoriasis. • Do not administer IV
or intramuscularly. • Rotate injection
PHARMACOKINETICS sites.
Degrades into small peptides, amino acids Storage • Store kit in refrigera-
via catabolic pathway. Primarily excreted tor. • Reconstituted solution should ap-
in urine. Bioavailability: 86–89% follow- pear as a clear, colorless to light straw-
ing SQ injection. Peak plasma concentra- colored liquid. • Discard if particulate
tion: 3–5 hrs. Half-life: 1.3–2 hrs. is present. • Drug should be com-
pletely dissolved before solution is with-
LIFESPAN CONSIDERATIONS drawn from vial.
Pregnancy/Lactation: Unknown INDICATIONS/ROUTES/DOSAGE
if distributed in breast milk. Chil-
Short Bowel Syndrome
dren: Safety and efficacy not estab-
lished. Elderly: No age-related precau- SQ: ADULTS/ELDERLY: 0.05 mg/kg once
tions noted. daily. CHILDREN 1 YR OR OLDER, WEIGHING
10 KG OR MORE: 0.05 mg/kg/dose. Maxi-
INTERACTIONS mum: 0.05 mg/dose.
DRUG: May increase concentration/ Dosage in Moderate to Severe Renal
effects of benzodiazepines (e.g., AL- T
Impairment
PRAZolam, LORazepam). HERBAL: SQ: ADULTS/ELDERLY: CrCl less than
None significant. FOOD: None known. 50 mL/min: 50% dose reduction.
LAB VALUES: None significant.
Dosage in Hepatic Impairment
AVAILABILITY (Rx) No dose adjustment.
Injection, Powder for Reconstitution:
5 mg (delivers maximum of 0.38 mL con- SIDE EFFECTS
taining 3.8 mg teduglutide). Frequent (30%–22%): Abdominal pain,
nausea, injection site reactions. Occa-
ADMINISTRATION/HANDLING sional (18%–14%): Headache, abdominal
SQ distention, vomiting. Rare (9%): Flatu-
Reconstitution • If diluent syringe lence, hypersensitivity, appetite disor-
(contains 0.5 mL Sterile Water for Injection) ders, sleep disturbances.

Canadian trade name Non-Crushable Drug High Alert drug


1124 telavancin

ADVERSE EFFECTS/TOXIC
REACTIONS telavancin
Upper respiratory tract infection occurs
tel-a-van-sin
in 12% of pts. Fluid overload (hypervol-
(Vibativ)
emia) reported in 7% of pts. Potential
for hypovolemia is increased in pts with j BLACK BOX ALERT jPts with
preexisting renal impairment (CrCl
cardiovascular disease, HF. Therapy less than 50 mL/min) who are treated
increases risk for acceleration for neo- for hospital-acquired pneumonia may
plastic growth. Cholecystitis, cholangitis, have increased mortality risk when
cholelithiasis, pancreatitis have been compared to vancomycin. May cause
reported. new or worsening renal impairment.
May cause fetal harm (low birth
weight, limb malformations). Women
NURSING CONSIDERATIONS of childbearing potential should have
BASELINE ASSESSMENT
pregnancy test before treatment;
avoid use during pregnancy unless
Obtain baseline serum chemistries, LFT, benefit to pt outweighs fetal risk.
lipase, amylase. Colonoscopy (or alter- Do not confuse telavancin with
nate imaging) with removal of polyps dalbavancin or oritavancin;
should be completed within 5 mos prior or Vibativ with Vibra-Tabs or
to initiating treatment. vigabatrin.
INTERVENTION/EVALUATION uCLASSIFICATION
Follow-up colonoscopy (or alternate PHARMACOTHERAPEUTIC: Lipo-
imaging) is recommended at the end of glycopeptide antibacterial. CLINI-
1 year. If no polyp is found, subsequent CAL: Antibiotic.
colonoscopies should be done no less
frequently than every 5 yrs. If a polyp
is found, adherence to current polyp USES
follow-up guidelines is recommended. Treatment of complicated skin, soft tissue
Discovery of intestinal obstruction, infections (cSSSI) caused by gram-posi-
intestinal malignancy necessitates dis- tive microorganisms, including methicil-
continuation of treatment. Subsequent lin-susceptible or methicillin-resistant S.
laboratory assessments, LFT are recom- aureus, vancomycin-susceptible Entero-
mended every 6 mos. If clinically mean- coccus. Treatment of hospital-acquired
ingful elevation is seen, further diagnos- and ventilator-associated bacterial pneu-
T tic workup is recommended as clinically monia (HABP/VABP) caused by suscep-
indicated. tible isolates of S. aureus.
PATIENT/FAMILY TEACHING
PRECAUTIONS
• Teach proper use and administration Contraindications: Prior hypersensitivity
of medication. • Be aware of need for reactions to telavancin. Concomitant use of
any new supplies. • Instruct pt in prep- IV unfractionated heparin. Cautions: Re-
aration of medication, and observe cor- nal impairment (CrCl 50 mL/min or less),
rect administration technique. • Re- concurrent therapy with other nephrotoxic
port yellowing of skin or eyes, dark medications (e.g., NSAIDs, ACE inhibi-
urine, changes in stool color or consis- tors, aminoglycosides). Avoid use in pts
tency, severe abdominal pain, nausea, with history of congenital QT syndrome,
vomiting, sudden weight gain, swelling, known prolongation of QT interval, un-
or difficulty breathing. compensated HF, severe left ventricular

underlined – top prescribed drug


telavancin 1125
hypertrophy, or receiving treatment with Reconstitution • Reconstitute with
other drugs known to prolong QT interval, 45 mL Sterile Water for Injection, D5W,
hypokalemia, hypomagnesemia, known or 0.9% NaCl to provide concentration of
vancomycin hypersensitivity. 15 mg/mL (total volume approximately
50 mL). • Prior to administration, fur-
ACTION ther dilute with D5W or 0.9% NaCl to final
Inhibits bacterial cell wall synthesis by concentration of 0.6–8 mg/mL. • Do
blocking polymerization and cross-link- not shake.
ing of peptidoglycan. Disrupts membrane Rate of administration • Infuse over
potential and changes cell wall permea- at least 60 min. Flush line with D5W or
bility. Therapeutic Effect: Bactericidal. 0.9% NaCl before and after administra-
Antibiotic. tion.
Storage • Discard if particulate is
PHARMACOKINETICS present. • Following reconstitution,
Not metabolized in liver; pathway un- drug is stable for 4 hrs at room tempera-
specified. Protein binding: 90%. Primar- ture or 72 hrs if refrigerated in vial or
ily excreted unchanged in urine. Not re- infusion bag.
moved by hemodialysis. Half-life: 8–9
hrs. IV INCOMPATIBILITIES
LIFESPAN CONSIDERATIONS Amphotericin, colistimethate, levoFLOXa-
cin (Levaquin), micafungin (Mycomine).
Pregnancy/Lactation: May cause fetal
harm at regular dosage. Unknown if dis- IV COMPATIBILITIES
tributed in breast milk. Children: Safety Azithromycin, caspofungin, cefepime,
and efficacy not established. El- cefTAZidime, cefTRIAXone, ciprofloxa-
derly: Age-related renal impairment cin, doripenem, doxycycline, gentamicin,
may increase risk of nephrotoxicity; dos- ertapenem, fluconazole, meropenem,
age adjustment recommended. tobramycin, pantoprazole, piperacillin-
INTERACTIONS tazobactam, tigecycline.
DRUG: QT interval–prolonging INDICATIONS/ROUTES/DOSAGE
medi­ cations (e.g., amiodarone, Usual Parenteral Dosage
azithromycin, ceritinib, haloperi- IV infusion: ADULTS, ELDERLY: 10 mg/
dol, moxifloxacin) may increase risk kg once every 24 hrs for 7–14 days
of QT interval prolongation, cardiac ar- (cSSSI); 14–21 days (HABP/VABP). Du-
rhythmias. May decrease therapeutic effect ration based on severity, infection site, T
of heparin. HERBAL: None significant. and clinical progress of pt.
FOOD: None known. LAB VALUES: May
alter serum potassium. May increase serum Dosage in Renal Impairment
bilirubin, ALT, AST, BUN, creatinine; PT, aPTT, Creatinine
INR. May decrease Hgb, Hct, WBC count. Clearance Dosage
AVAILABILITY (Rx) 50 mL/min or 10 mg/kg every 24 hrs
greater
Injection, Powder for Reconstitution: 30–49 mL/min 7.5 mg/kg every 24 hrs
750 mg. 10–29 mL/min 10 mg/kg every 48 hrs
Less than No dose adjustment
ADMINISTRATION/HANDLING 10 mL/min (not studied)
IV

b ALERT c Give by intermittent IV infu- Dosage in Hepatic Impairment


sion (piggyback). Do not give by IV push No dose adjustment (unless concomitant
(may result in hypotension). renal impairment).

Canadian trade name Non-Crushable Drug High Alert drug


1126 telmisartan

SIDE EFFECTS
Frequent (33%–27%): Altered taste,
telmisartan
nausea. Occasional (14%–6%): Vomit-
tel-mi-sar-tan
ing, foamy urine, diarrhea, dizziness,
(Apo-Telmisartan , Micardis)
pruritus. Rare (4%–2%): Rigors, rash,
infusion site pain, anorexia, infusion site j BLACK BOX ALERT jMay
cause fetal injury, mortality. Dis-
erythema. continue as soon as possible once
pregnancy is detected.
ADVERSE EFFECTS/TOXIC
REACTIONS FIXED-COMBINATION(S)
Nephrotoxicity (acute kidney injury, Micardis HCT: telmisartan/hydro-
acute tubular necrosis, renal failure), CHLOROthiazide (a diuretic): 40
diarrhea due to C. difficile may occur. mg/12.5 mg, 80 mg/12.5 mg. Twynsta:
“Red-man syndrome” (characterized by telmisartan/amLODIPine (a calcium
erythema on face, neck, upper torso), channel blocker): 40 mg/5 mg, 40
tachycardia, hypotension, myalgia, an- mg/10 mg, 80 mg/5 mg, 80 mg/10 mg.
gioedema may occur from too-rapid
rate of infusion. May cause QT interval uCLASSIFICATION
prolongation. PHARMACOTHERAPEUTIC: Angio-
tensin II receptor antagonist. CLINI-
NURSING CONSIDERATIONS CAL: Antihypertensive.
BASELINE ASSESSMENT
Obtain pregnancy test prior to treat- USES
ment. Obtain baseline serum BUN,
creatinine, creatinine clearance prior Treatment of hypertension alone or in
to initiating therapy, every 48–72 hrs, combination with other antihyperten-
and after treatment is completed. Obtain sives. Reduces cardiovascular risk in pts
culture and sensitivity tests before giv- 55 yrs of age and older unable to take
ing first dose (therapy may begin before ACE inhibitors and at high risk of major
results are known). Question history of cardiovascular event (e.g., MI, stroke).
renal impairment, long QT interval syn- PRECAUTIONS
drome, HF.
Contraindications: Hypersensitivity to
INTERVENTION/EVALUATION telmisartan. Concurrent use with aliski-
Monitor renal function tests, I&O. As- ren in pts with diabetes. Cautions: Hy-
T
sess skin for rash. Avoid rapid infusion povolemia, hyperkalemia, hepatic/
(“red-man syndrome”). Monitor daily renal impairment, renal artery stenosis
pattern of bowel activity, stool consis- (unilateral, bilateral), biliary obstruc-
tency. Obtain C. difficile PCR test if tive disease, significant aortic/mitral
diarrhea occurs. Monitor ECG for QT stenosis. Concurrent use with ramipril
interval prolongation, cardiac arrhyth- not recommended. Avoid potassium
mias. supplements.
PATIENT/FAMILY TEACHING ACTION
• Use effective contraception during Blocks vasoconstrictor and aldosterone-
treatment. • Report rash, signs/symp- secreting effects of angiotensin II, in-
toms of nephrotoxicity, diarrhea. • Blood hibiting binding of angiotensin II to AT1
levels will be monitored routinely. • Re- receptors. Therapeutic Effect: Causes
port chest pain, irregular heart rhythm, vasodilation, decreases peripheral resis-
palpitations, passing out. tance, decreases B/P.

underlined – top prescribed drug


telotristat ethyl 1127

PHARMACOKINETICS SIDE EFFECTS


Route Onset Peak Duration Occasional (7%–3%): Upper respiratory
PO (reduce B/P) 1–2 hrs — 24 hrs tract infection, sinusitis, back/leg pain,
diarrhea. Rare (1%): Dizziness, head-
Rapidly, completely absorbed. Protein ache, fatigue, nausea, heartburn, myal-
binding: greater than 99%. Metabolized gia, cough, peripheral edema.
in liver. Excreted in feces. Unknown if re-
moved by hemodialysis. Half-life: 24 hrs. ADVERSE EFFECTS/TOXIC
REACTIONS
LIFESPAN CONSIDERATIONS Overdosage may manifest as hypoten-
Pregnancy/Lactation: May cause fetal sion, tachycardia; bradycardia occurs
harm. Unknown if drug is distributed in less often.
breast milk. Children: Safety and ef-
ficacy not established. Elderly: No age- NURSING CONSIDERATIONS
related precautions noted.
BASELINE ASSESSMENT
INTERACTIONS Obtain B/P, apical pulse immediately
DRUG: NSAIDs (e.g., ibuprofen, ketoro- before each dose, in addition to regular
lac, naproxen) may increase adverse effects. monitoring (be alert to fluctuations). If
May increase lithium concentration, risk of excessive reduction in B/P occurs, place
toxicity. Aliskiren may increase hyperkale- pt in supine position, feet slightly ele-
mic effect. May increase adverse effect/toxicity vated. Assess medication history (esp. di-
of ACE inhibitors (e.g., benazepril, lisin- uretics). Question for history of hepatic/
opril, ramipril). HERBAL: Herbals with renal impairment, renal artery stenosis.
hypertensive properties (e.g., licorice, Obtain serum BUN, creatinine, Hgb, Hct,
yohimbe) or hypotensive properties vital signs (particularly B/P, pulse rate).
(e.g., garlic, ginger, ginkgo biloba) may INTERVENTION/EVALUATION
alter effects. FOOD: None known. LAB VAL-
UES: May increase serum BUN, creatinine,
Monitor B/P, pulse, serum electrolytes,
uric acid, cholesterol. May decrease Hgb, Hct. renal function. Monitor for hypotension
when initiating therapy.
AVAILABILITY (Rx)
PATIENT/FAMILY TEACHING
Tablets: 20 mg, 40 mg, 80 mg.
• Avoid tasks that require alertness, mo-
ADMINISTRATION/HANDLING tor skills until response to drug is estab-
lished (possible dizziness effect). •
PO
Maintain proper hydration. • Avoid preg- T
• Give without regard to food.
nancy. • Immediately report suspected
INDICATIONS/ROUTES/DOSAGE pregnancy. • Report any sign of infection
Hypertension (sore throat, fever). • Avoid excessive
PO: ADULTS, ELDERLY: Initially, 20–40 exertion during hot weather (risk of dehy-
mg once daily. Titrate based on pt’s re- dration, hypotension).
sponse up to 80 mg once daily.
Cardiovascular Risk Reduction
PO: ADULTS, ELDERLY: 80 mg once daily. telotristat ethyl
Dosage in Renal Impairment
No dose adjustment. tel-oh-tri-state eth-il
(Xermelo)
Dosage in Hepatic Impairment Do not confuse telotristat with
Use with caution. Triostat, or Xermelo with Xarelto.

Canadian trade name Non-Crushable Drug High Alert drug


1128 telotristat ethyl
uCLASSIFICATION INTERACTIONS
PHARMACOTHERAPEUTIC: Trypto- DRUG: Octreotide may decrease con-
phan hydroxylase inhibitor. CLINI- centration/effect (give short-acting
CAL: GI agent. octreotide at least 30 min after telotri-
stat ethyl). HERBAL: None significant.
FOOD: High-fat meals increases
USES drug exposure. LAB VALUES: May in-
Treatment of carcinoid syndrome diar- crease alkaline phosphatase, ALT, AST,
rhea in combination with somatostatin GGT.
analog (SSA) therapy in adults with
symptoms inadequately controlled by SSA AVAILABILITY (Rx)
therapy. Tablets: 250 mg.
PRECAUTIONS ADMINISTRATION/HANDLING
Contraindications: Hypersensitivity to PO
telotristat, telotristat ethyl. Cautions: Pts • Give with food. • If applicable, give
with advanced carcinoid tumors may short-acting octreotide at least 30 mins
be at risk for altered structural integ- after telotristat ethyl. • If a dose is
rity of the GI wall. Conditions that may missed, do not give extra dose. Adminis-
impair integrity of GI wall (e.g., Crohn’s ter next dose at regularly scheduled
disease, diverticulitis, GI tract malig- time.
nancies, intestinal adhesions, Ogilvie’s
syndrome, peptic ulcers, peritoneal ma- INDICATIONS/ROUTES/
lignancies). DOSAGE
Carcinoid Syndrome Diarrhea
ACTION PO: ADULTS, ELDERLY: 250 mg 3 times/
Inhibits enzyme tryptophan hydroxylase day.
(TPH). TPH converts tryptophan to 5-hy-
droxytryptophan, and then to serotonin, Dosage in Renal Impairment
reducing overproduction and biosynthe- Creatinine clearance greater that 20
sis of peripheral serotonin. Therapeutic mL/min: No dose adjustment. ESRD
Effect: Reduces frequency of carcinoid requiring hemodialysis: Not studied;
syndrome diarrhea. use caution.

PHARMACOKINETICS Dosage in Hepatic Impairment


T Does not cross blood-brain barrier. Un- Mild impairment: No dose adjustment.
dergoes hydrolysis via carboxylesterases Moderate to severe impairment: Not
to active metabolite telotristat. Protein studied; use caution.
binding: greater than 99%. Peak plasma
concentration: 1–3 hrs (telotristat). Ex-
SIDE EFFECTS
creted in feces (93%), urine (less than Occasional (13%–5%): Nausea, headache,
1%). Half-life: 5 hrs (telotristat). peripheral edema, flatulence, decreased
appetite, pyrexia, abdominal pain, ab-
LIFESPAN CONSIDERATIONS dominal distension, constipation.
Pregnancy/Lactation: Unknown
if crosses placenta or distributed in ADVERSE EFFECTS/TOXIC
breast milk. May increase risk of constipa- REACTIONS
tion in nursing infants. Children: Safety Severe constipation resulting in GI per-
and efficacy not established. Elderly: No foration, bowel obstruction may occur.
age-related precautions noted. Depression reported in 9% of pts.

underlined – top prescribed drug


temozolomide 1129

NURSING CONSIDERATIONS lesions, cutaneous T-cell lymphomas,


advanced neuroendocrine tumors, soft
BASELINE ASSESSMENT tissue sarcoma, pediatric neuroblastoma.
Question characteristics of diarrhea, Ewing’s sarcoma (recurrent or progres-
frequency of bowel movements. Assess sive).
bowel sounds. Question history of GI
obstruction, GI perforation, baseline GI PRECAUTIONS
disease. Assess hydration status. Contraindications: Hypersensitivity to
temozolomide, dacarbazine. Cau-
INTERVENTION/EVALUATION tions: Severe renal/hepatic impairment,
Assess bowel sounds. Monitor for severe, pregnancy.
persistent, or worsening of abdominal
pain. Discontinue if severe constipation, ACTION
severe abdominal pain, GI perforation, Produces cytotoxic effect through alkyla-
bowel obstruction occurs. Monitor daily tion of DNA, causing DNA double strand
pattern of bowel activity, stool consis- breaks and apoptosis. Therapeutic Ef-
tency. fect: Inhibits DNA replication, causing
cell death.
PATIENT/FAMILY TEACHING
PHARMACOKINETICS
• Take with food. • Immediately re-
port severe, persistent abdominal pain; Rapidly, completely absorbed after PO
abdominal distension, fever, nausea, administration. Protein binding: 15%.
vomiting; may indicate tear or blockage Peak plasma concentration: 1 hr. Pen-
in GI tract. • Report severe constipa- etrates blood-brain barrier. Excreted
tion. • Do not breastfeed. • If therapy in urine (38%), feces (19%). Half-
includes somatostatin, take somatostatin life: 1.6–1.8 hrs.
at least 30 mins after dose. LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: May cause
fetal harm. May produce malformation
temozolomide of external organs, soft tissue, skeleton.
If possible, avoid use during pregnancy.
tem-oh-zoe-loe-myde Unknown if drug is distributed in breast
(Temodal , Temodar) milk. Children: Safety and efficacy not
Do not confuse Temodar with established. Elderly: Pts older than 70
Tambocor. yrs may experience higher risk of de- T
veloping Grade 4 neutropenia, Grade 4
uCLASSIFICATION thrombocytopenia.
PHARMACOTHERAPEUTIC: Imidazo- INTERACTIONS
tetrazine derivative, alkylating agent.
CLINICAL: Antineoplastic. DRUG: Valproic acid may increase
adverse effects. Bone marrow de-
pressants (e.g., cladribine) may
USES increase myelosuppression. Live vi-
Treatment of adults with refractory ana- rus vaccines may potentiate virus
plastic astrocytoma, newly diagnosed replication, increase vaccine side ef-
glioblastoma multiforme (concomitantly fects, decrease pt’s antibody response
with radiotherapy, then as maintenance to vaccine. HERBAL: Echinacea may
therapy). OFF-LABEL: Malignant glioma, decrease effects. FOOD: All foods
metastatic melanoma, metastatic CNS decrease rate, extent of drug absorp-
tion. LAB VALUES: May decrease Hgb,

Canadian trade name Non-Crushable Drug High Alert drug


1130 temozolomide
neutrophils, platelets, WBC count, lym- logic toxicity Grade 1 or less. Mainte-
phocytes. nance phase: (begin 4 wks after con-
comitant phase completion): (Cycle
AVAILABILITY (Rx) 1): 150 mg/m2 once daily for 5 days
Capsules: 5 mg, 20 mg, 100 mg, 140 followed by 23 days without treatment.
mg, 180 mg, 250 mg. Injection, Powder (Cycles 2–6): May increase to 200 mg/
for Reconstitution: 100 mg. m2 once daily for 5 days followed by 23
days without treatment if ANC greater than
ADMINISTRATION/HANDLING 1,500 cells/mm3, platelets greater than
IV 100,000 cells/mm3, and nonhematologic
toxicity with previous cycle is Grade 2 or
• Reconstitute each 100-mg vial with 41 less (exclude alopecia, nausea, vomiting).
mL Sterile Water for Injection to provide
concentration of 2.5 mg/mL. • Swirl Dosage in Renal/Hepatic Impairment
gently; do not shake. • Do NOT further No dose adjustment. Use caution in se-
dilute. • Infuse over 90 min. • Stable vere hepatic impairment.
for 14 hrs (includes infusion time).
SIDE EFFECTS
PO Frequent (53%–33%): Nausea, vomiting,
• Food reduces rate, extent of absorption; headache, fatigue, constipation, seizure.
increases risk of nausea, vomiting. • For Occasional (16%–10%): Diarrhea, asthe-
best results, administer at bedtime. • Give nia, fever, dizziness, peripheral edema,
capsule whole with glass of water. Do not incoordination, insomnia. Rare (9%–
break, open, or crush capsules. 5%): Paresthesia, drowsiness, anorexia,
INDICATIONS/ROUTES/DOSAGE urinary incontinence, anxiety, pharyngi-
tis, cough.
Anaplastic Astrocytoma (Refractory)
IV infusion, PO: ADULTS, ELDERLY: Ini- ADVERSE EFFECTS/TOXIC
tially, 150 mg/m2/day for 5 consecu- REACTIONS
tive days of 28-day treatment cycle. Myelosuppression is characterized by
Subsequent doses of 100–200 mg/m2/ neutropenia and thrombocytopenia, with
day based on platelet count, absolute elderly pts and women showing higher
neutrophil count (ANC) during previ- incidence of developing severe myelo-
ous cycle. Maintenance: 200 mg/m2/ suppression. Usually occurs within first
day for 5 days q4wks if ANC greater than few cycles; is not cumulative. Nadir oc-
1,500 cells/mm3 and platelets more than curs in approximately 26–28 days, with
T
100,000 cells/mm3. Continue until dis- recovery within 14 days of nadir. May
ease progression is observed. Minimum: increase occurrence of Pneumocystis
100 mg/m2/day for 5 days q4wks. carinii pneumonia, myelodysplastic syn-
Glioblastoma Multiforme
drome including myeloid leukemia, or
Note: Pneumocystis carinii pneu- secondary malignancies.
monia (PCP) prophylaxis required dur- NURSING CONSIDERATIONS
ing concomitant phase and continue in
pts who develop lymphocytopenia until BASELINE ASSESSMENT
recovery to Grade 1 or less. IV infu- Obtain baseline CBC. Before dosing, ANC
sion, PO: ADULTS, ELDERLY: Concomitant must be greater than 1,500 cells/mm3
phase: 75 mg/m2 daily for 42 days (with and platelet count greater than 100,000
focal radiotherapy) if ANC 1,500 cells/ cells/mm3. Potential for nausea, vomit-
mm3 or greater, platelet count 100,000 ing (readily controlled with antiemetic
cells/mm3 or greater, and nonhemato- therapy). Offer emotional support.

underlined – top prescribed drug


temsirolimus 1131
INTERVENTION/EVALUATION medication that may cause angioedema
Obtain CBC on day 22 (21 days after (e.g., ACE inhibitors).
first dose) or within 48 hrs of that day,
and wkly, until ANC is greater than 1,500 ACTION
cells/mm3 and platelet count is greater Prevents activation of mTOR (mecha-
than 100,000 cells/mm3. Monitor for nistic target of rapamycin), preventing
hematologic toxicity (fever, sore throat, tumor cell division. Therapeutic Ef-
signs of local infection, unusual bruis- fect: Inhibits tumor cell growth, pro-
ing/bleeding from any site), symptoms duces tumor regression.
of anemia (excessive fatigue, weakness).
PHARMACOKINETICS
PATIENT/FAMILY TEACHING Metabolized in liver. Excreted primarily
• To reduce nausea/vomiting, take on in feces. Half-life: 17 hrs.
an empty stomach at bed-
time. • Promptly report fever, sore LIFESPAN CONSIDERATIONS
throat, signs of local infection, unusual Pregnancy/Lactation: May cause fetal
bruising/bleeding from any site, or diffi- harm. Unknown if distributed in breast
culty breathing. • Avoid crowds, those milk. Children: Safety and efficacy not
with infection. • Do not have immuni- established. Elderly: No age-related
zations without physician’s ap- precautions noted.
proval. • Avoid pregnancy.
INTERACTIONS
DRUG: CYP3A4 inhibitors (e.g.,
clarithromycin, ketoconazole, rito-
temsirolimus navir) may increase concentration/
effect. CYP3A4 inducers (e.g., car-
tem-sir-oh-li-mus BAMazepine, phenytoin, rifAMPin)
(Torisel) may decrease concentration/effect. May
Do not confuse temsirolimus decrease the therapeutic effect; increase
with everolimus, sirolimus, or adverse effects of vaccines (live).
tacrolimus. HERBAL: St. John’s wort may decrease
uCLASSIFICATION plasma concentration/effect. Echina-
cea may decrease the therapeutic effect.
PHARMACOTHERAPEUTIC: mTOR FOOD: Grapefruit products may in-
kinase inhibitor. CLINICAL: Antineo- crease plasma concentration/effect. LAB
plastic. VALUES: May increase serum bilirubin, T
alkaline phosphatase, AST, creatinine, glu-
USES cose, cholesterol, triglycerides. May de-
crease WBCs, neutrophils, Hgb, platelets,
Treatment of advanced renal cell carci- serum phosphorus, potassium.
noma.
PRECAUTIONS AVAILABILITY (Rx)
Injection Solution Kit: 25 mg/mL sup-
Contraindications:Hypersensitivity to
plied with 1.8-mL diluent vial.
temsirolimus. Moderate-severe hepatic
impairment; serum bilirubin greater than
1.5 times upper limit of normal (ULN).
ADMINISTRATION/HANDLING
Cautions: Hypersensitivity to sirolimus, IV
mild hepatic impairment, diabetes, hy- Reconstitution • Inject 1.8 mL of di-
perlipidemia. Concurrent use with other luent into vial. • The vial contains an

Canadian trade name Non-Crushable Drug High Alert drug


1132 temsirolimus
overfill of 0.2 mL (30 mg/1.2 mL). • Due Dosage in Hepatic Impairment
to the overfill, the drug concentration of Mild impairment: Reduce dose to 15
resulting solution will be 10 mg/mL. • A mg/wk. Moderate to severe impair-
total volume of 3 mL will be obtained, in- ment: Contraindicated.
cluding the overfill. • Mix well by invert-
ing the vial. Allow sufficient time for air SIDE EFFECTS
bubbles to subside. • Mixture must be Common (51%–32%): Asthenia, rash, mu-
injected rapidly into 250 mL 0.9% cositis, nausea, edema (facial edema,
NaCl. • Invert bag to mix; avoid exces- peripheral edema), anorexia. Frequent
sive shaking (may cause foaming). (28%–20%): Generalized pain, dyspnea,
Rate of administration • Administer diarrhea, cough, fever, abdominal pain,
through an in-line filter not greater than constipation, back pain, impaired taste.
5 microns; infuse over 30–60 min. • Fi- Occasional (19%–8%): Weight loss, vom-
nal diluted infusion solution should be iting, pruritus, chest pain, headache, nail
completed within 6 hrs from the time disorder, insomnia, nosebleed, dry skin,
drug solution and diluent mix- acne, chills, myalgia.
ture is added to the 250 mL 0.9% NaCl.
Storage • Refrigerate kit. • Recon- ADVERSE EFFECTS/TOXIC
stituted solution appears clear to slightly REACTIONS
turbid, colorless to yellow, and free from UTI occurs in 15% of pts, hypersensitivity
visible particulates. • The 10 mg/mL reaction in 9%, pneumonia in 8%, upper
drug solution/diluent mixture is stable respiratory tract infection, hypertension,
for up to 24 hrs at room tempera- conjunctivitis in 7%.
ture. • Solutions diluted for infusion
(in 250 mL 0.9% NaCl) must be infused NURSING CONSIDERATIONS
within 6 hrs of preparation. BASELINE ASSESSMENT

IV INCOMPATIBILITIES Question possibility of pregnancy. Obtain


baseline CBC, serum chemistries, renal
Both acids and bases degrade solution; function, LFT routinely thereafter. Offer
combinations of temsirolimus with emotional support.
agents capable of modifying solution pH
should be avoided. INTERVENTION/EVALUATION
Offer antiemetics to control nausea, vom-
INDICATIONS/ROUTES/DOSAGE iting. Monitor daily pattern of bowel fre-
b ALERT c Pretreat with IV diphen- quency, stool consistency. Assess skin for
T hydrAMINE 25–50 mg, 30 min before evidence of rash, edema. Monitor CBC,
infusion. particularly Hgb, platelets, neutrophil
count; LFT, renal function tests. Monitor
Renal Cancer
for shortness of breath, fatigue, hyperten-
IV: ADULTS/ELDERLY: 25 mg once wkly. sion. Assess oropharynx for stomatitis,
Treatment should continue until disease mucositis.
progresses or unacceptable toxicity oc-
curs. PATIENT/FAMILY TEACHING
• Avoid crowds, those with known infec-
Dose Modification
tion. • Avoid contact with anyone who
Concomitant CYP3A4 inhibi-
recently received live virus vac-
tors: Consider dose of 12.5 mg/
cine. • Do not have immunizations
wk. Concomitant CYP3A4 induc- without physician’s approval (drug low-
ers: Consider dose of 50 mg/wk.
ers body resistance). • Promptly report
Dosage in Renal Impairment fever, unusual bruising/bleeding from
No dose adjustment. any site.

underlined – top prescribed drug


teriflunomide 1133

PHARMACOKINETICS
teriflunomide Well absorbed following PO administra-
tion. Peak concentration: 1–4 hrs. Protein
ter-i-floo-noe-myde
binding: greater than 99%. Metabolized by
(Aubagio)
hydrolysis. Excreted in urine (23%), feces
j BLACK BOX ALERT j May (38%). Half-life: 18–19 days.
result in major birth defects.
Pregnancy must be excluded before
initiating therapy and must be LIFESPAN CONSIDERATIONS
avoided during treatment or prior to Pregnancy/Lactation: May produce
completion of an accelerated elimi-
nation procedure. Severe hepatic embryo-fetal toxicity. Pregnancy contra-
injury may occur. Do not initiate with indicated. Avoid breastfeeding. Detected
acute/chronic liver disease or serum in human semen. Children: Safety and
ALT greater than 2 times upper limit efficacy not established. Elderly: No
of normal. age-related precautions noted.
Do not confuse teriflunomide
with leflunomide. INTERACTIONS
uCLASSIFICATION DRUG: May increase concentration/ef-
fects of CYP2C8 substrates (e.g., re-
PHARMACOTHERAPEUTIC: Py-
paglinide, PACLitaxel, rosuvastatin,
rimidine synthesis inhibitor, immu-
topotecan). May decrease concentration/
nomodulatory agent. CLINICAL: Mul-
effects of warfarin, CYP1A2 substrates
tiple sclerosis agent.
(e.g., DULoxetine, tiZANidine). May
decrease the therapeutic effect; increase ad-
verse effects of vaccines (live). HERBAL:
USES Echinacea may decrease the therapeutic
Treatment of relapsing forms of multiple effect. FOOD: None known. LAB VAL-
sclerosis. UES: May increase serum potassium, ALT,
AST, alkaline phosphatase, bilirubin. May
PRECAUTIONS decrease WBCs, neutrophil count.
Contraindications: Hypersensitivity to ter-
iflunomide, leflunomide. Pregnant women AVAILABILITY (Rx)
or women of childbearing potential who Tablets: 7 mg, 14 mg.
are not using reliable contraception, se-
vere hepatic impairment, concurrent use ADMINISTRATION/HANDLING
of leflunomide. Cautions: Concomitant PO T
neurotoxic medications, diabetes, pulmo- • Give without regard to food.
nary disease, severe immunodeficiency or
bone marrow dysplasia, history of signifi- INDICATIONS/ROUTES/DOSAGE
cant hematologic abnormalities, uncon- Multiple Sclerosis
trolled infection, history of new/recurrent PO: ADULTS, ELDERLY: 7 mg or 14 mg
infections, pts older than 60 yrs. once daily.

ACTION Adjustment of Toxicity


Inhibits pyrimidine synthesis, exhibiting ALT elevation greater than 3 times ULN:
anti-inflammatory and antiproliferative Discontinue teriflunomide and initi-
properties. Therapeutic Effect: May ate drug elimination procedures: cho-
reduce number of activated lymphocytes lestyramine 8 g q8h for 11 days (if not
in the CNS. May slow progression of mul- tolerated, may decrease to 4 g q8h) or
tiple sclerosis. activated charcoal 50 g q12h for 11 days.
Note: The 11 days do not need to be

Canadian trade name Non-Crushable Drug High Alert drug


1134 teriparatide
consecutive unless plasma concentration tion of treatment must be considered.
needs to be lowered rapidly. If drug-induced hepatic impairment,
peripheral neuropathy, severe skin reac-
Dosage in Renal Impairment tion occur, discontinue medication, begin
No dose adjustment. accelerated elimination procedure (chole-
styramine or charcoal for 11 days). Moni-
Dosage in Hepatic Impairment tor for symptom improvement of MS.
Mild to moderate impairment: No
PATIENT/FAMILY TEACHING
dose adjustment. Severe impair-
ment: Contraindicated. • Women of childbearing potential must
be counseled regarding fetal risk, use of
SIDE EFFECTS reliable contraceptives confirmed, possi-
Frequent (19%–6%): Headache, diar-
bility of pregnancy excluded. • May
rhea, nausea, alopecia, paresthesia, take without regard to food. • Report
upper abdominal pain. Occasional (4%– symptoms of infection such as body
3%): ­Hypertension, oral herpes, anxiety,
aches, chills, cough, fatigue, fever.
hypertension, toothache, musculoskel-
etal pain. Rare (2%–1%): Seasonal al-
lergy, sciatica, burning sensation, carpal
tunnel syndrome, blurred vision, acne, teriparatide
pruritus, myalgia, abdominal distention,
conjunctivitis. ter-i-par-a-tide
(Forteo)
ADVERSE EFFECTS/TOXIC j BLACK BOX ALERT jIncreased
risk of osteosarcoma; risk depend-
REACTIONS ent on dose and duration.
Influenza occurs in 12% of pts, up-
per respiratory infection with sinusitis, uCLASSIFICATION
bronchitis in 9%. Cystitis, sinusitis, viral PHARMACOTHERAPEUTIC: Parathy-
gastroenteritis may occur. Neutropenia, roid hormone. CLINICAL: Osteopo-
leukopenia occur rarely. rosis agent.
NURSING CONSIDERATIONS
USES
BASELINE ASSESSMENT
Treatment of postmenopausal women
Because of high potential for birth de-
T with osteoporosis who are at increased
fects/fetal death, female pts must avoid
risk for fractures. Treatment of men with
pregnancy. Obtain baseline PPD for latent
primary or hypogonadal osteoporosis
TB. Obtain CBC, hepatic function test re-
who are at high risk for fractures. High-
sults prior to treatment and monthly for
risk pts include those with a history of
6 mos thereafter. Obtain baseline preg-
osteoporotic fractures, who have failed
nancy test. Assess baseline symptoms
previous osteoporosis therapy, or were
of MS (e.g., bladder/bowel dysfunction,
intolerant of previous osteoporosis ther-
cognitive impairment, depression, dys-
apy. Treatment of glucocorticoid-induced
phagia, fatigue, gait disorder, numbness/
osteoporosis in men and women.
tingling, pain, seizures, spasticity, trem-
ors, weakness). PRECAUTIONS
INTERVENTION/EVALUATION Contraindications: Hypersensitivity to
Monitor for signs/symptoms of infec- ter­ipa­ratide. Cautions: Conditionsthat
tion. Treatment should not be initiated increase risk of osteosarcoma (e.g.,
if pt has active infection; discontinua- Paget’s disease, unexplained elevations

underlined – top prescribed drug


testosterone 1135
of alkaline phosphatase level, children INDICATIONS/ROUTES/DOSAGE
or young adults with open epiphyses, Osteoporosis
prior skeletal radiation therapy, implant SQ: ADULTS, ELDERLY: 20 mcg once
therapy), hypercalcemia, hypercalcemic daily into thigh, abdominal wall. Continue
disorders (e.g., hyperparathyroidism), for up to 2 yrs (lifetime duration).
bone metastases, history of skeletal
malignancies, metabolic bone diseases Dosage in Renal/Hepatic Impairment
other than osteoporosis, cardiac disease, No dose adjustment.
renal/hepatic impairment, pts at risk for
orthostasis, active or recent urolithiasis. SIDE EFFECTS
Occasional: Leg cramps, nausea, dizzi-
ACTION ness, headache, orthostatic hypotension,
Stimulates osteoblast function. Increases tachycardia.
calcium absorption from GI tract/renal
tubular reabsorption. Therapeutic Ef- ADVERSE EFFECTS/TOXIC
fect: Increases bone mineral density, REACTIONS
bone mass/strength, reduces osteoporo- Angina pectoris has been reported.
sis-related fractures.
NURSING CONSIDERATIONS
PHARMACOKINETICS
BASELINE ASSESSMENT
Extensively absorbed following SQ injec-
tion. Metabolized in liver. Excreted in Obtain urinary, serum calcium, ion-
urine. Half-life: 1 hr. ized calcium levels, serum parathy-
roid hormone levels, bone mineral
LIFESPAN CONSIDERATIONS density.
Pregnancy/Lactation: Unknown if INTERVENTION/EVALUATION
drug crosses placenta or is distributed Monitor bone mineral density, urinary/
in breast milk. Children: Safety and ef- serum calcium levels, serum parathy-
ficacy not established. Elderly: No age- roid hormone levels. Observe for symp-
related precautions noted. toms of hypercalcemia. Monitor B/P
INTERACTIONS for hypotension, pulse for tachycardia.
Question medical history as listed in
DRUG: None significant. HERBAL: None Precautions.
significant. FOOD: None known. LAB
VALUES: May increase serum calcium PATIENT/FAMILY TEACHING
(transient), uric acid. • Go from lying to standing slowly. • T
Report persistent symptoms of hypercal-
AVAILABILITY (Rx) cemia (nausea, vomiting, constipation,
Injection Solution:600 mcg/2.4 mL (in- lethargy, asthenia).
jector pen containing 28 daily doses of
20 mcg).
ADMINISTRATION/HANDLING testosterone
SQ
• Refrigerate, but minimize time out of tes-tos-te-rone
refrigerator. Do not freeze; discard if (Andriol , Androderm, AndroGel
frozen. • Administer into thigh, abdom- Pump, Aveed, Depo-Testosterone,
inal wall. Fortesta, Natesto, Striant, Testim,
Testopel, Vogelxo)

Canadian trade name Non-Crushable Drug High Alert drug


1136 testosterone

j BLACK BOX ALERT j LIFESPAN CONSIDERATIONS


Virilization in children and women
may occur following secondary Pregnancy/Lactation: Contraindi-
exposure to testosterone topical cated in pregnant women, women who
gel and solution. Aveed: Serious may become pregnant, or during lac-
pulmonary oil microembolism tation. Children: Safety and efficacy
reaction and anaphylaxis reported not established; use with caution. El-
during or immediately after admin-
istration. derly: May increase risk of hyperpla-
Do not confuse testosterone sia, stimulate growth of occult prostate
with testolactone. carcinoma.

uCLASSIFICATION INTERACTIONS
PHARMACOTHERAPEUTIC: Andro- DRUG: May increase hepatotoxic effect
gen. CLINICAL: Sex hormone. of cycloSPORINE. May increase the an-
ticoagulant effect of warfarin. HERBAL:
None significant. FOOD: None known.
USES LAB VALUES: May increase Hgb, Hct,
Androgen replacement therapy in treat- LDL, serum alkaline phosphatase, bili-
ment of delayed male puberty, male hy- rubin, calcium, potassium, sodium, AST.
pogonadism (congenital or acquired), May decrease HDL.
inoperable female breast cancer pts who
are 1–5 yrs postmenopausal. AVAILABILITY (Rx)
Gel, Topical: (AndroGel, Testim): 1%,
PRECAUTIONS 1.62%. (Vogelxo): 50-mg packet or tube,
Contraindications:Hypersensitivity to 12.5 mg/actuation metered dose pump.
testosterone. Breastfeeding, pregnant (Fortesta): 10 mg/actuation. Injection:
or who may become pregnant, prostate (Cypionate [Depo-Testosterone]): 100
(known or suspected) or breast cancer mg/mL, 200 mg/mL. (Enanthate [Delat-
in males. Depo-Testosterone (ad- estryl]): 200 mg/mL. (Aveed [Undecano-
ditional): Severe cardiac/hepatic/re- ate]): 750 mg/3 mL. Mucoadhesive, for
nal disease. Cautions: Renal/hepatic/ Buccal Application: (Striant): 30 mg.
cardiac dysfunction, pts with history Nasal Gel: (Natesto): 5.5 mg/actuation.
of MI or CAD; conditions influenced Pellet for SQ Implantation: 12.5 mg, 25
by edema (e.g., seizure disorder, mi- mg, 37.5 mg, 50 mg, 75 mg. Solution,
graines). Metered Dose Pump: (Axiron): 30 mg/
activation. Transdermal System Patch:
T
ACTION (Androderm): 2 mg/day or 4 mg/day.
Promotes growth, development of male
sex organs, maintains secondary sex ADMINISTRATION/HANDLING
characteristics in androgen-deficient IM
males. Therapeutic Effect: Relieves • Give deep in gluteal muscle. • Do
androgen deficiency. not give IV. • Warming or shaking re-
dissolves crystals that may form in
PHARMACOKINETICS long-acting preparations. • Wet nee-
Well absorbed after IM administration. dle of syringe may cause solution to
Protein binding: 98%. Metabolized in become cloudy; this does not affect
liver. Primarily excreted in urine. Un- potency.
known if removed by hemodialysis.
Buccal
­Half-life: 10–100 min.
• (Striant):Apply to gum area (above
incisor tooth). • Hold firmly in place

underlined – top prescribed drug


testosterone 1137
for 30 sec to ensure adhesion. Instruct pt Topical gel: (Fortesta): 40 mg once
to not chew or swallow. • Not affected daily in morning. Range: 10–70 mg.
by food, toothbrushing, gum, chewing, Maximum: 70 mg. (Vogelxo): 50 mg
alcoholic beverages. • Remove before once daily (one tube or one packet or 4
placing new system. pump actuations).
Topical solution: (Axiron): ADULTS,
Transdermal ELDERLY: 60 mg once daily (1 pump ac-
• (Androderm): Apply to clean, dry area tivation of 30 mg to each axilla). Range:
on skin on back, abdomen, upper arms, 30–120 mg.
thighs. • Do not use tape to secure. Transdermal patch: (Androderm):
Avoid bathing, swimming for at least ADULTS, ELDERLY: Start therapy with 4
3 hrs after each application. • Do mg/day patch applied at night. Apply
not apply to bony prominences (e.g., patch to abdomen, back, thighs, upper
shoulder) or oily, damaged, irritated arms. Dose adjustment based on testos-
skin. Do not apply to scrotum. • Ro- terone levels. Range: 2–6 mg/day.
tate application site with 7-day interval Transdermal gel: ADULTS, ELDERLY:
to same site. (AndroGel 1%): Initial dose of 5 g deliv-
ers 50 mg testosterone and is applied once
Transdermal Gel
daily to abdomen, shoulders, upper arms.
• (AndroGel, Testim, Vogelxo): Apply May increase to 7.5 g (75 mg testoster-
(morning preferred) to clean, dry, in- one), then to 10 g (100 mg testosterone),
tact skin of shoulder, upper arms. (An- if necessary. (AndroGel 1.62%): Initial
droGel 1% may also be applied to ab- dose of 40.5 mg applied once daily in the
domen.) • Upon opening packet(s), morning to shoulder and upper arms. May
squeeze entire contents into palm of increase to 81 mg. Further adjustments
hand, immediately apply to application based on testosterone levels.
site. • Allow to dry. • Do not apply to Transdermal gel: (Testim, Vogelxo):
genitals. • (Fortesta): Apply to skin of ADULTS, ELDERLY: Initial dose of 5 g deliv-
front and inner thighs. ers 50 mg testosterone and is applied once
Topical Solution daily to the shoulders, upper arms. May in-
• (Axiron): Apply using applicator to ax- crease to 10 g (100 mg testosterone).
illa at same time each morning. • Avoid Buccal: (Striant): ADULTS, ELDERLY: 30
washing site for 2 hrs after application. mg q12h.
Nasal gel: (Natesto): ADULTS EL-
INDICATIONS/ROUTES/DOSAGE DERLY: 11 mg (2 actuations, 1 per each
Male Hypogonadism nostril) 3 times/day (6–8 hrs apart). T
IM: ADULTS: (Enanthate): 75–100 mg/ Delayed Male Puberty
wk or 150–200 mg q2wks. (Undecano- IM: (Cypionate or Enanthate): ADO-
ate): 750 mg at initiation, 4 wks and
LESCENTS: 50–200 mg q2–4wks for lim-
q10 wks thereafter. CHILDREN 12 YRS AND ited duration (4–6 months).
OLDER: (Cypionate or Enanthate): Ini-
SQ: (Pellets): ADULTS: 150–450 mg
tiation of pubertal growth: 25–75 mg q3– q3–6mos.
4wks, gradually titrate q6–9mos to 100–
150 mg. Duration: 3–4yrs. Maintenance Breast Carcinoma
virilizing dose: 200–250 mg q3–4wks. IM: (Testosterone Cypionate, Testos-
May convert to other testosterone re- terone Ethanate): ADULTS: 200–400 mg
placement dosages once expected adult q2–4wks.
height and adequate virilization achieved.
SQ: (Pellets): ADULTS, CHILDREN 12 YRS Dosage in Renal/Hepatic Impairment
AND OLDER: 150–450 mg q3–6mos. Use caution.

Canadian trade name Non-Crushable Drug High Alert drug


1138 tiaGABine

SIDE EFFECTS adequate intake of protein, calories.


Frequent: Gynecomastia, acne. Fe- Assess for virilization. Monitor sleep
males: Hirsutism, amenorrhea, other patterns. Monitor for CVA (aphasia,
menstrual irregularities; deepening of confusion, paresthesia, hemiparesis,
voice; clitoral enlargement (may not seizures), MI (chest pain, diaphoresis,
be reversible when drug is discontin- left arm/jaw pain, increased serum tro-
ued). Occasional: Edema, nausea, in- ponin, ST segment elevation), pulmo-
somnia, oligospermia, priapism, male- nary embolism (chest pain, dyspnea,
pattern baldness, bladder irritability, hypoxia, tachycardia).
hypercalcemia (in immobilized pts, PATIENT/FAMILY TEACHING
those with breast cancer), hypercho-
• Regular visits to physician and moni-
lesterolemia, inflammation/pain at IM
toring tests are necessary. • Do not
injection site. Transdermal: Pruritus,
take any other medication without con-
erythema, skin irritation. Rare: Poly-
sulting physician. • Maintain diet high
cythemia (with high dosage), hyper-
in protein, calories. • Food may be
sensitivity.
better tolerated in small, frequent feed-
ADVERSE EFFECTS/TOXIC ings. • Weigh daily; report 5 lb/wk
REACTIONS gain. • Report nausea, vomiting, acne,
pedal edema. • Females: Promptly
Peliosis hepatitis (presence of blood-
report menstrual irregularities, hoarse-
filled cysts in parenchyma of liver),
ness, deepening of voice. • Males:
hepatic neoplasms, hepatocellular
Report frequent erections, difficulty uri-
carcinoma have been associated with
nating, gynecomastia. • Treatment
prolonged high-dose therapy. Anaphy-
may cause arterial or venous blood
lactic reactions occur rarely. Venous
clots; report symptoms of heart attack
thromboembolism (e.g., DVT, PE) re-
(chest pain, difficulty breathing, jaw
ported.
pain, nausea, pain that radiates to the
NURSING CONSIDERATIONS left arm, sweating), stroke (blindness,
confusion, one-sided weakness, loss of
BASELINE ASSESSMENT consciousness, trouble speaking, sei-
Establish baseline weight, B/P, Hgb, Hct. zures); DVT (swelling, pain, hot feeling
Check LFT, electrolytes, cholesterol. Wrist in the arms or legs), lung embolism
X-rays may be ordered to determine bone (difficulty breathing, chest pain, rapid
maturation in children. Question history heart rate).
T of hepatic/renal impairment, seizure
disorder, thromboembolism (CVA, MI,
pulmonary embolism).
INTERVENTION/EVALUATION
tiaGABine
Weigh daily, report wkly gain of more tye-a-ga-been
than 5 lb; evaluate for edema. Moni- (Gabitril)
tor I&O. Monitor B/P. Assess serum Do not confuse tiaGABine with
electrolytes, cholesterol, Hgb, Hct tiZANidine.
(periodically for high dosage), LFT,
radiologic exam of wrist, hand (when uCLASSIFICATION
using in prepubertal children). With PHARMACOTHERAPEUTIC: Selec-
breast cancer or immobility, check for tive GABA reuptake inhibitor. CLINI-
hypercalcemia (lethargy, muscle weak- CAL: Anticonvulsant.
ness, confusion, irritability). Ensure

underlined – top prescribed drug


tiaGABine 1139

USES INDICATIONS/ROUTES/DOSAGE
Adjunctive therapy for treatment of par- Note: Pts not taking enzyme-inducing an-
tial seizures in adults and children 12 yrs tiepileptic drugs (AEDs): Lower doses re-
or older. quired and slower titration may be needed.
Do not use a loading dose, rapid titration,
PRECAUTIONS and/or increase in large-dose increments.
Contraindications: Hypersensitivity to ti-
aGABine. Cautions: Hepatic impairment. Partial Seizures
Pts at risk for suicidal behavior/thoughts. PO: ADULTS, ELDERLY: Pts receiving en-
zyme-inducing AED regimens: Initially,
ACTION 4 mg once daily. May increase by 4–8 mg/
Enhances activity of gamma-aminobu- day at wkly intervals. Maintenance: 32–56
tyric acid (GABA), the major inhibitory mg/day in 2–4 divided doses. CHILDREN 12–
neurotransmitter in the CNS. Therapeu- 18 YRS: Pts receiving enzyme-inducing
tic Effect: Inhibits seizure activity. AED regimens: Initially, 4 mg once daily
for 1 wk. May increase by 4 mg in 2 divided
PHARMACOKINETICS doses for 1 wk, then may increase by 4–8 mg
Rapidly absorbed from GI tract. Protein at wkly intervals thereafter. Maximum: 32
binding: 96%. Metabolized in liver. Primar- mg/day in 2–4 divided doses.
ily excreted in feces. Half-life: 2–5 hrs. Dosage in Renal Impairment
LIFESPAN CONSIDERATIONS No dose adjustment.
Pregnancy/Lactation: May produce Dosage in Hepatic Impairment
teratogenic effects. Distributed in breast Use caution.
milk. Children: Safety and efficacy not
established in pts younger than 12 yrs. SIDE EFFECTS
Elderly: Age-related hepatic impair- Frequent (34%–20%): Dizziness, asthenia
ment may require dosage adjustment. (loss of strength, energy), drowsiness, ner-
vousness, confusion, headache, infection,
INTERACTIONS tremor. Occasional: Nausea, diarrhea, ab-
DRUG: CNS depressants (e.g., alco- dominal pain, impaired concentration.
hol, morphine, oxyCODONE, zol-
pidem) may increase CNS depression. ADVERSE EFFECTS/TOXIC
Strong CYP3A4 inducers (e.g., carBA- REACTIONS
Mazepine, phenytoin, rifAMPin) may Overdose characterized by agitation, con-
decrease concentration/effect. Strong fusion, hostility, weakness. Full recovery T
CYP3A4 inhibitors (e.g., clarithromy- occurs within 24 hrs of discontinua-
cin, ketoconazole) may increase con- tion. Depression, suicidal ideation.
centration/effect. HERBAL: Herbals with
sedative properties (e.g., chamomile, NURSING CONSIDERATIONS
kava kava, valerian) may increase CNS BASELINE ASSESSMENT
depression. St. John’s wort may de-
crease concentration/effect. FOOD: None Review history of seizure disorder (inten-
known. LAB VALUES: None significant. sity, frequency, duration, level of conscious-
ness). Observe frequently for recurrence of
AVAILABILITY (Rx) seizure activity. Initiate seizure precautions.
Tablets: 2 mg, 4 mg, 12 mg, 16 mg. INTERVENTION/EVALUATION
For pts on long-term therapy, serum hepatic/
ADMINISTRATION/HANDLING renal function tests, CBC should be per-
• Give with food. formed periodically. Assist with ambulation if

Canadian trade name Non-Crushable Drug High Alert drug


1140 ticagrelor
dizziness occurs. Assess for clinical improve- hepatic impairment. Cautions: Moder-
ment (decrease in intensity, frequency of ate hepatic impairment, renal impair-
seizures). Monitor for depression, unusual ment, history of hyperuricemia or gouty
behavior, suicidal ideation or thoughts. arthritis. Pts at increased risk of brady-
cardia, concurrent use of strong CYP3A4
PATIENT/FAMILY TEACHING
inhibitors or inducers, elderly pts. (Rec-
• Go from lying to standing ommend holding dose 5 days before
slowly. • Avoid tasks that require alert- planned surgery if applicable.) Pts with
ness, motor skills until response to drug risk factors for bleeding (e.g., trauma,
is established. • Avoid alcohol. • Re- peptic ulcer disease).
port worsening seizure activity, thoughts
of suicide, increased depression. ACTION
Reversibly inhibits platelet P2Y12 ADP
receptor to prevent signal transduction
ticagrelor and platelet activation. Therapeutic Ef-
fect: Reduces platelet aggregation.
tye-ka-grel-or
(Brilinta) PHARMACOKINETICS
j BLACK BOX ALERT jMay cause Readily absorbed after PO administration.
significant, sometimes fatal bleeding. Protein binding: 99%. Metabolized in
Do not use with active bleeding or
history of intracranial bleeding. Do liver. Primarily excreted in feces (58%),
not initiate in pts planning urgent urine (26%). Half-life: 7–9 hrs.
coronary artery bypass graft (CABG)
surgery. Discontinue at least 5 days LIFESPAN CONSIDERATIONS
prior to any surgery. Suspect bleed- Pregnancy/Lactation: Unknown if
ing in any pt who is hypotensive
and has had recent percutaneous distributed in breast milk. Must either
coronary intervention (PCI), CABG, discontinue breastfeeding or discontinue
or other surgical procedures. If drug therapy. Children: Safety and ef-
possible, manage bleeding without ficacy not established. Elderly: No age-
discontinuing therapy to decrease related precautions noted.
risk of cardiovascular events. Aspirin
maintenance doses greater than 100 INTERACTIONS
mg/day may reduce effectiveness
and should be strictly avoided. DRUG: Aspirin greater than 100 mg/day
may decrease effectiveness. CYP3A4 in-
uCLASSIFICATION hibitors (e.g., clarithromycin, keto-
T PHARMACOTHERAPEUTIC: P2Y 12 conazole) may increase concentration/
platelet aggregation inhibitor. CLINI- effects. CYP3A4 inducers (e.g., car-
CAL: Antiplatelet. BAMazepine, phenytoin, rifAMPin)
may decrease concentration/effects. An-
ticoagulants (e.g., warfarin), anti-
USES platelets (e.g., aspirin, clopidogrel),
Reduce rate of cardiovascular death, MI, NSAIDs (e.g., ibuprofen, ketorolac,
stroke in pts with acute coronary syn- naproxen) may increase risk of bleeding.
drome (ACS) or history of MI. Reduce May increase adverse effects of apixaban,
rate of stent thrombosis in pts who have dabigatran, edoxaban. May increase
been stented for treatment of ACS. concentration of digoxin, simvastatin,
lovastatin. HERBAL: St. John’s wort may
PRECAUTIONS decrease concentration/effect. Herbals
Contraindications: Hypersensitivity to with anticoagulant/antiplatelet prop-
ticagrelor. History of intracranial hemor- erties (e.g., garlic, ginger, ginkgo
rhage, active pathologic bleeding, severe biloba), glucosamine may increase risk

underlined – top prescribed drug


tigecycline 1141
of bleeding. FOOD: Grapefruit products NURSING CONSIDERATIONS
may increase potential for bleeding. LAB
VALUES: May increase serum uric acid, BASELINE ASSESSMENT
creatinine. Obtain CBC, serum chemistries, renal func-
tion, LFT. Question for history of bleeding,
AVAILABILITY (Rx) stomach ulcers, colon polyps, head trauma,
Tablets: 60 mg, 90 mg. cardiac arrhythmias, unstable angina, re-
cent MI, hepatic impairment, hypertension,
ADMINISTRATION/HANDLING stroke. Receive full medication history in-
PO cluding herbal products. Question for his-
• Give without regard to food. • May tory of COPD, chronic bronchitis, emphy-
be crushed, mixed with water, and drunk sema, asthma, exertional dyspnea.
immediately (refill glass with water, stir
and drink contents). INTERVENTION/EVALUATION
Routinely screen for bleeding. Assess
INDICATIONS/ROUTES/DOSAGE skin for bruising, hematoma. Monitor
Acute Coronary Syndrome renal function, uric acid, digoxin levels if
PO: ADULTS: Initially, 180 mg once, applicable. Report hematuria, epistaxis,
then 90 mg twice daily. (begin 12h af- coffee-ground emesis, black/tarry stools.
ter initial loading dose). Give with aspi- Monitor ECG for chest pain, shortness of
rin 325 mg once (loading dose), then breath, syncope.
maintain with aspirin 75–100 mg daily. PATIENT/FAMILY TEACHING
Continue for up to 12 mos, then decrease
dose to 60 mg twice daily. • It may take longer to stop bleeding dur-
ing therapy. • Do not vigorously blow
Dosage in Renal Impairment nose. • Use soft toothbrush, electric razor
No dose adjustment. to decrease risk of bleeding. • Immedi-
ately report bloody stool, urine, or nose-
Dosage in Hepatic Impairment bleeds. • Report all newly prescribed
Mild impairment: No dose adjust- medications. • Inform physician of any
ment. Moderate impairment: Use cau- planned dental procedures or surgeries.
tion. Severe impairment: Avoid use.
SIDE EFFECTS
Occasional (13%–7%): Dyspnea, head- tigecycline
ache. Rare (5%–3%): Cough, dizziness,
nausea, diarrhea, back pain, fatigue. tye-gee-sye-kleen T
(Tygacil)
ADVERSE EFFECTS/TOXIC
REACTIONS j BLACK BOX ALERT j An
increase in all-cause mortality ob-
Life-threatening events including intra- served in Phase 3 and 4 clinical tri-
cranial bleeding, epistaxis, intrapericar- als. Use is reserved when alternate
treatment is not appropriate.
dial bleeding with cardiac tamponade,
hypovolemic shock requiring vasopres- uCLASSIFICATION
sive support or blood transfusion re-
PHARMACOTHERAPEUTIC: Glycylcy-
ported. Pts with history of sick sinus syn-
drome, second- or third-degree AV block, cline. CLINICAL: Antibiotic.
bradycardic syncope have increased risk
of bradycardia. May induce episodes of USES
atrial fibrillation, hypotension, hyperten-
Treatment of susceptible infections due
sion. Gynecomastia reported in less than
to E. coli, E. faecalis, S. aureus, S. aga-
1% of men.
Canadian trade name Non-Crushable Drug High Alert drug
1142 tigecycline
lactiae, S. anginosus group (includes S. known. LAB VALUES: May increase se-
anginosus, S. intermedius, S. constella- rum alkaline phosphatase, amylase, BUN,
tus), S. pyogenes, B. fragilis, Citrobac- bilirubin, glucose, LDH, ALT, AST. May de-
ter freundii, E. cloacae, K. oxytoca, K. crease Hgb, WBCs, thrombocytes, serum
pneumoniae, B. thetaiotaomicron, B. potassium, protein.
uniformis, B. vulgatus, C. perfringens,
Peptostreptococcus micros including AVAILABILITY (Rx)
complicated skin/skin structure infec- Injection, Powder for Reconstitution: (Ty-
tions, complicated intra-abdominal in- gacil): 50-mg vial.
fections, community-acquired bacterial
pneumonia. ADMINISTRATION/HANDLING
PRECAUTIONS IV
Contraindications: Hypersensitivity to Reconstitution • Add 5.3 mL 0.9%
tigecycline. Cautions: Hypersensitivity
to NaCl or D5W to each 50-mg vial. • Swirl
tetracyclines, pregnancy, hepatic impair- gently to dissolve. • Resulting solution
ment, monotherapy for pts with intesti- is 10 mg/mL. • Immediately withdraw
nal perforation. Do not use for diabetic 5 mL reconstituted solution and add to
foot infections, healthcare (hospital)- 100 mL 0.9% NaCl or D5W bag for infu-
acquired pneumonia, or ventilator-asso- sion (final concentration should not ex-
ciated pneumonia. ceed 1 mg/mL).
Rate of administration • Administer
ACTION over 30–60 min every 12 hrs. • May be
Inhibits protein synthesis by binding to given through a dedicated line or piggy-
ribosomal receptor sites of bacterial cell back. If same line is used for sequential
wall. Therapeutic Effect: Bacterio- infusion of several different drugs, line
static effect. should be flushed before and after infusion
of tigecycline with either 0.9% NaCl or D5W.
PHARMACOKINETICS Storage • Reconstituted solution is sta­
Extensive tissue distribution, minimally ble for up to 6 hrs at room temperature or
metabolized. Excreted by biliary/fecal up to 24 hrs if refrigerated. • Reconsti-
route (59%), urine (33%). Protein tuted solution appears yellow to red-or-
binding: 71%–89%. Half-life: Single ange. • Discard if solution is discolored
dose: 27 hrs; following multiple doses: (green, black) or precipitate forms.
42 hrs.
T IV INCOMPATIBILITIES
LIFESPAN CONSIDERATIONS Amphotericin B, methylPREDNISolone,
Pregnancy/Lactation: May cause fetal voriconazole.
harm. May be distributed in breast milk.
Permanent discoloration of the teeth IV COMPATIBILITIES
(brown-gray) may occur if used during Amikacin, azithromycin, aztreonam,
tooth development. Children: Safety and cefepime, cefTAZidime, ciprofloxacin,
efficacy not established in pts younger doripenem, ertapenem, fluconazole,
than 8 yrs. Use is reserved for when no ef- gentamicin, linezolid, piperacillin-tazo-
fective alternative is available. Elderly: No bactam, potassium chloride, telavancin,
age-related precautions noted. tobramycin, vancomycin.
INTERACTIONS INDICATIONS/ROUTES/DOSAGE
DRUG: May increase concentration Systemic Infections
of warfarin, increase bleeding time. Ini-
IV: ADULTS OVER 18 YRS, ELDERLY:
HERBAL: None significant. FOOD: None tially, 100 mg, followed by 50 mg
underlined – top prescribed drug
tildrakizumab-asmn 1143
every 12 hrs for 5–14 days. CHILDREN 12
YRS AND OLDER: 50 mg q12h. CHILDREN tildrakizumab-asmn
8–11 YRS: 1.2–2 mg/kg q12h. Maxi-
mum: 50 mg/dose. til-dra-kiz-ue-mab-asmn
(Ilumya)
Dosage in Renal Impairment Do not confuse tildrakizumab-
No dose adjustment. asmn with atezolizumab, ben-
ralizumab, certolizumab, dacli-
Dosage in Hepatic Impairment zumab, eculizumab, efalizumab,
Mild to moderate impairment: No mepolizumab, tositumomab, or
dose adjustment in mild to moderate trastuzumab.
impairment. Severe impairment:
IV: ADULTS OVER 18 YRS, ELDERLY: Ini- uCLASSIFICATION
tially, 100 mg, followed by 25 mg every PHARMACOTHERAPEUTIC: Interleu-
12 hrs. kin-23 antagonist. Monoclonal anti-
body. CLINICAL: Antipsoriatic agent.
SIDE EFFECTS
Frequent (29%–13%): Nausea, vomiting,
diarrhea. Occasional (7%–4%): Head- USES
ache, hypertension, dizziness, in- Treatment of moderate to severe plaque
creased cough, delayed healing. Rare psoriasis in adults who are candidates for
(3%–2%): Peripheral edema, pruritus, systemic therapy or phototherapy.
constipation, dyspepsia, asthenia (loss of
strength, energy), hypotension, phlebitis, PRECAUTIONS
insomnia, rash, diaphoresis. Contraindications: Hypersensitivity to til-
drakizumab-asmn. Cautions: Conditions
ADVERSE EFFECTS/TOXIC predisposing to infection (e.g., diabetes,
REACTIONS immunocompromised pts, renal failure,
Dyspnea, abscess, pseudomembranous open wounds), prior exposure to tuber-
colitis (abdominal cramps, severe watery culosis. Concomitant use of live vaccines
diarrhea, fever) ranging from mild to not recommended.
life-threatening may result from altered
ACTION
bacterial balance in GI tract.
Selectively binds to p19 subunit of in-
NURSING CONSIDERATIONS terleukin-23 (IL-23) and inhibits in-
teraction with IL-23 receptor. IL-23 is a
BASELINE ASSESSMENT cytokine that is involved in inflammatory T
Obtain baseline CBC, hepatic function and immune response. Therapeutic Ef-
test. Question for history of allergies, esp. fect: Alters biologic immune response;
tetracyclines, before therapy. reduces inflammation.
INTERVENTION/EVALUATION PHARMACOKINETICS
Monitor daily pattern of bowel activity, Widely distributed. Degraded into small
stool consistency. Be alert for super- peptides and amino acids via catabolic
infection: fever, anal/genital pruritus, pathway. Peak plasma concentration:
oral mucosal changes (ulceration, pain, 6 days. Steady state reached in 16 wks.
erythema). Nausea, vomiting may be con- Half-life: 23 days.
trolled by antiemetics.
PATIENT/FAMILY TEACHING
LIFESPAN CONSIDERATIONS
• Report diarrhea, rash, mouth sore- Pregnancy/Lactation: Unknown if
ness, other new symptoms. distributed in breast milk. However, hu-
man immunoglobulin G (IgG) is present
Canadian trade name Non-Crushable Drug High Alert drug
1144 tildrakizumab-asmn
in breast milk and is known to cross the Dosage in Renal /Hepatic Impairment
placenta. Children: Safety and efficacy Not specified; use caution.
not established. Elderly: No age-related
precautions noted. SIDE EFFECTS
Rare (3%–2%): Injection site reactions
INTERACTIONS (bruising, edema, erythema, hematoma,
DRUG: May decrease therapeutic effect hemorrhage, inflammation, pain, pruri-
of live vaccines. May increase risk of tus, swelling, urticaria), diarrhea.
adverse effects/toxic reactions of beli-
mumab, live vaccines. HERBAL: None ADVERSE EFFECTS/TOXIC
significant. FOOD: None known. LAB REACTIONS
VALUES: None known. Hypersensitivity reactions including an-
gioedema, urticaria may occur. Upper re-
AVAILABILITY (Rx) spiratory tract infections reported in 14%
Injection Solution, Prefilled Syringe: 100 of pts. Infections reported in 23% of pts.
mg/mL. May increase risk of serious infecti­ons.
Immunogenicity (auto-tildrakizumab-
ADMINISTRATION/HANDLING asmn antibodies) occurred in 7% of pts.
SQ
Preparation • Remove prefilled sy- NURSING CONSIDERATIONS
ringe from refrigerator and allow solu- BASELINE ASSESSMENT
tion to warm to room temperature (ap-
prox. 30 mins) with needle cap Consider completion of immuniza-
intact. • Visually inspect for particulate tions before initiation. Pts should be
matter or discoloration. Solution should evaluated for active tuberculosis and
appear clear to slightly opalescent, color- tested for latent infection before ini-
less to slightly yellow in color. Do not use tiation and periodically during therapy.
if solution is cloudy, discolored, or if Induration of 5 mm or greater with tu-
visible particles are observed. • If pres- berculin skin testing should be consid-
ent, air bubbles do not need to be re- ered a positive test result when assess-
moved before administration. ing if treatment for latent tuberculosis
Administration • Insert needle sub- is necessary. Screen for active infection.
cutaneously into upper arms, outer thigh, Question history of chronic infections,
or abdomen and inject solution. • Do hypersensitivity reactions. Conduct der-
not inject into areas of active skin disease matologic exam; record characteristics
T or injury such as sunburns, skin rashes, of psoriatic lesions.
inflammation, skin infections, or active INTERVENTION/EVALUATION
psoriasis. • Do not administer IV or
intramuscular. • Rotate injection sites. Assess skin for improvement of lesions.
Storage • Refrigerate prefilled syringes Monitor for symptoms of tuberculosis,
in original carton until time of use. • Pro- including those who tested negative for
tect from light. • May store at room tem- latent tuberculosis infection before initiat-
perature for up to 30 days. Once warmed to ing therapy. Interrupt or discontinue treat-
room temperature, do not place back into ment if serious infection, opportunistic
refrigerator. • Do not freeze or expose to infection, or sepsis occurs. Monitor for
heating sources. • Do not shake. hypersensitivity reaction, angioedema.

INDICATIONS/ROUTES/DOSAGE PATIENT/FAMILY TEACHING

Plaque Psoriasis • Treatment may depress your immune


SQ: ADULTS, ELDERLY: 100 mg at wk 0 system and reduce your ability to fight
and wk 4, then q12wks thereafter. infection. Report symptoms of infection

underlined – top prescribed drug


tiotropium 1145
such as body aches, burning with urina- tors in bronchial smooth muscle. Thera-
tion, chills, cough, fatigue, fever. Avoid peutic Effect: Causes bronchodilation.
those with active infection. • Do not
receive live vaccines. • Expect frequent PHARMACOKINETICS
tuberculosis screening. • Report travel Binds extensively to tissue. Protein bind-
plans to possible endemic areas. • Re- ing: 72%. Metabolized by oxidation. Ex-
port allergic reactions such as itching, creted in urine. Half-life: 5–6 days.
swelling of the face or tongue.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown
if distributed in breast milk. Chil-
tiotropium dren: Safety and efficacy not established.
Elderly: Higher frequency of dry mouth,
tye-oh-trope-ee-yum constipation, UTI noted with increasing age.
(Spiriva HandiHaler, Spiriva
Respimat) INTERACTIONS
Do not confuse Spiriva with DRUG: Concurrent administration with
Inspra, or tiotropium with anticholinergics (e.g., aclidinium,
ipratropium. umeclidinium, ipratropium) may
increase adverse effects. HERBAL: None
FIXED-COMBINATION(S) significant. FOOD: None known. LAB
Stiolto Respimat: tiotropium/olo- VALUES: None significant.
daterol (a bronchodilator): 2.5 mcg/
2.5 mcg. AVAILABILITY (Rx)
Inhalation Spray: (Spiriva Respimat): 1.25
uCLASSIFICATION mcg/actuation, 2.5 mcg/actuation. Pow-
PHARMACOTHERAPEUTIC: An- der for Inhalation: (Spiriva): 18 mcg/cap-
ticholinergic (long-acting). CLINI- sule (in blister packs).
CAL: Bronchodilator.
ADMINISTRATION/HANDLING
Inhalation
USES
• (Spiriva): Open dustcap of Handi-
Long-term maintenance treatment of bron- Haler by pulling it upward, then open
chospasm associated with COPD, including mouthpiece. • Place capsule in cen-
chronic bronchitis, emphysema, and for ter chamber and firmly close mouth-
reducing COPD exacerbations. Spiriva piece until a click is heard, leaving the T
Respimat only: Maintenance treatment of dustcap open. • Hold HandiHaler
asthma in pts 6 yrs and older. device with mouthpiece upward, press
piercing button completely in once,
PRECAUTIONS
and release. • Instruct pt to breathe
Contraindications: Hypersensitivity to out completely before breathing in
tiotropium. History of hypersensitivity slowly and deeply but at rate sufficient
to ipratropium. Cautions: Narrow-angle to hear the capsule vibrate. • Have
glaucoma, prostatic hypertrophy, bladder pt hold breath as long as it is comfort-
neck obstruction, moderate to severe re- able until exhaling slowly. • Instruct
nal impairment, history of hypersensitiv- pt to repeat once again to ensure full
ity to atropine, myasthenia gravis. dose is received. • (Spiriva Respi-
mat): Refer to manufacturer’s pt in-
ACTION
structions.
Competitively and reversibly inhibits ac- Storage • Store at room temperature.
tion of acetylcholine at muscarinic recep- Do not expose capsules to extreme tem-
Canadian trade name Non-Crushable Drug High Alert drug
1146 tipiracil/trifluridine
perature, moisture. • Do not store cap- rales. Monitor ABGs. Observe for clavicu-
sules in HandiHaler device. • Use im- lar retractions, hand tremor. Evaluate for
mediately once foil is peeled back or clinical improvement (quieter, slower
removed. respirations, relaxed facial expression,
cessation of clavicular retractions).
INDICATIONS/ROUTES/DOSAGE
PATIENT/FAMILY TEACHING
COPD (Maintenance Treatment, Reduction
of COPD Exacerbations) • Increase fluid intake (decreases lung
Inhalation: ADULTS, ELDERLY: (Spiriva): secretion viscosity). • Do not use more
18 mcg (1 capsule)/day via HandiHaler in- than 1 capsule for inhalation in a 24h pe-
halation device. (Spiriva Respimat [2.5 riod. • Rinsing mouth with water imme-
mcg/actuation]): 2 inhalations (2.5 mg/ diately after inhalation may prevent mouth/
inhalation) once daily. throat dryness, thrush. • Avoid excessive
use of caffeine derivatives (chocolate, cof-
Asthma fee, tea, cola, cocoa). • Report eye pain/
Inhalation: ADULTS, ELDERLY, CHILDREN discomfort, blurred vision, visual halos.
6 YRS AND OLDER: (Spiriva Respimat
[1.25 mcg/actuation]): 2 inhalations
of 1.25 mcg once daily. Maximum benefit
may take up to 4–8 wks. tipiracil/trifluridine
Dosage in Renal Impairment trye-flure-i-deen/tye-pir-a-sil
CrCl 60 mL/min or less: Use caution (Lonsurf)
in moderate to severe impairment. Do not confuse trifluridine with
floxuridine, or tipiracil with
Dosage in Hepatic Impairment
tipifarnib or Pipracil.
No dose adjustment.
uCLASSIFICATION
SIDE EFFECTS
PHARMACOTHERAPEUTIC: Antime-
Frequent (16%–6%): Dry mouth, sinusitis, tabolite/thymidine phosphorylase
pharyngitis, dyspepsia, UTI, rhinitis. Oc- inhibitor. CLINICAL: Antineoplastic.
casional (5%–4%): Abdominal pain, pe-
ripheral edema, constipation, epistaxis,
vomiting, myalgia, rash, oral candidiasis. USES
Treatment of pts with metastatic colorectal
ADVERSE EFFECTS/TOXIC cancer who have been previously treated
T REACTIONS with fluoropyrimidine-, oxaliplatin-, and
Angina pectoris, depression, flu-like irinotecan-based chemotherapy, an anti–
symptoms, glaucoma, increased intra- vascular endothelial growth factor (VEGF)
ocular pressure occur rarely. biological therapy, and if RAS wild-type,
an anti–epidermal growth factor (EGFR)
NURSING CONSIDERATIONS therapy. Treatment of metastatic gastric or
BASELINE ASSESSMENT gastroesophageal junction adenocarcinoma
Question history of glaucoma, bladder previously treated with a fluoropyrimidine, a
outlet obstruction, renal impairment, my- platinum, and either a taxane or irinotecan.
asthenia gravis. Auscultate lung sounds.
PRECAUTIONS
INTERVENTION/EVALUATION Contraindications: Hypersensitivity to triflu-
Monitor rate, depth, rhythm, type of ridine or tipiracil. Cautions: Baseline ane-
respiration; quality, rate of pulse. As- mia, leukopenia, neutropenia, thrombocy-
sess lung sounds for rhonchi, wheezing, topenia; active infection, pts at increased

underlined – top prescribed drug


tipiracil/trifluridine 1147
risk of infection (e.g., diabetes, indwelling ADMINISTRATION/HANDLING
catheters), pts with high tumor burden, his- PO
tory of pulmonary embolism; pregnancy, • Give within 1 hr of completion of
moderate to severe hepatic impairment. morning and evening meals. Do not give
on empty stomach.
ACTION
Trifluridine (active cytotoxic component) INDICATIONS/ROUTES/DOSAGE
interferes with DNA synthesis and cell Note: Do not initiate the cycle until ANC is
proliferation of cancer cells. Tipiracil 1,500 cells/mm3 or greater; febrile neutro-
increases exposure of trifluridine by in- penia is resolved; platelet count is 75,000
hibiting metabolism via thymidine phos- cells/mm3 or greater; Grade 3 or 4 nonhe-
phorylase. Therapeutic Effect: Inhib- matologic toxicity is resolved to Grade 1 or 0.
its tumor cell growth and metastasis.
Colorectal, Gastric Cancer
PHARMACOKINETICS PO: ADULTS, ELDERLY: (Dose based on tri-
Rapidly absorbed. Metabolized by thymidine fluridine component) 35 mg/m2 (rounded
phosphorylase (not metabolized in liver). Pro- to nearest 5-mg increment) twice daily on
tein binding: trifluridine: 96%; tipiracil: 8%. days 1–5 and days 8–12 of 28-day cycle.
Peak plasma concentration: 2 hrs. Excreted Continue until disease progression or un-
primarily in urine (50%). Half-life: trifluri- acceptable toxicity. Maximum: 80 mg/
dine: 1.4 hrs (2.1 hrs at steady state); tipiracil: dose (based on trifluridine component).
2.1 hrs (2.4 hrs at steady state).
Dose Modification
Based on Common Terminology Criteria
LIFESPAN CONSIDERATIONS
for Adverse Events (CTCAE).
Pregnancy/Lactation: Avoid preg-
nancy; may cause fetal harm. Female Hematologic/Nonhematologic Toxicity
pts of reproductive potential must use Interrupt treatment for ANC less than
effective contraception during treat- 500 cells/mm3; febrile neutropenia;
ment. Unknown if distributed in breast platelet count less than 50,000 cells/
milk. Breastfeeding not recommended. mm3; Grade 3 or 4 nonhematologic tox-
Males: Due to risk of potential icity. Do not restart until ANC is 1,500
­exposure, male pts must use condoms cells/mm3 or greater; febrile neutrope-
during sexual activity during treatment nia is resolved; platelet count is 75,000
and up to 3 mos after discontinuation. cells/mm3 or greater; Grade 3 or 4 non-
Children: Safety and efficacy not estab- hematologic toxicity is resolved to Grade T
lished. Elderly: May have increased risk 1 or 0 (except Grade 3 nausea and/or
of neutropenia, thrombocytopenia. vomiting controlled by antiemetic ther-
apy; Grade 3 diarrhea responsive to an-
INTERACTIONS tidiarrheal medication). Once resolved,
DRUG: May decrease therapeutic effect; in- resume at decreased incremental dose
crease adverse effects of vaccines (live). of 5 mg/m2 from previous dose. A maxi-
HERBAL: Echinacea may decrease thera- mum of 3 dose reductions is allowed
peutic effect. FOOD: None known. LAB to dosage minimum of 20 mg/m2 twice
VALUES: Expected to decrease Hct, Hgb, daily. Do not increase dose after it has
platelets, neutrophils, RBC, WBC. been reduced.
AVAILABILITY (Rx) Dosage in Renal Impairment
Fixed-Dose Combination Tablets: (Tri- Mild to moderate impairment: No
fluridine/Tipiracil): 15 mg/6.14 mg, 20 dose adjustment. Severe impair-
mg/8.19 mg. ment: Not studied; use caution.

Canadian trade name Non-Crushable Drug High Alert drug


1148 tisagenlecleucel
Dosage in Hepatic Impairment Monitor for bleeding if thrombocytope-
Mild impairment: No dose adjust- nia occurs.
ment. Moderate to severe impair-
ment: Not studied; use caution. PATIENT/FAMILY TEACHING
• Blood levels will be monitored regu-
SIDE EFFECTS larly. • Treatment may cause fetal harm.
Frequent (52%–19%): Asthenia, fatigue, Female pts of childbearing potential
nausea, diarrhea, decreased appetite, should use effective contraception during
vomiting, abdominal pain, pyrexia. Oc- treatment. Immediately report suspected
casional (8%–7%): Stomatitis, dysgeusia, pregnancy. Do not breastfeed. • Male
alopecia. pts must use condoms during sexual activ-
ity. • Immediately report chest pain, dif-
ADVERSE EFFECTS/TOXIC ficult breathing, fast heart rate, rapid
REACTIONS breathing; may indicate life-threatening
Severe and/or life-threatening myelosup- blood clot in the lungs. • Report symp-
pression including anemia (77% of pts), toms of bone marrow suppression or in-
Grade 3 anemia (18% of pts), neutro- fection such as bruising easily, chills,
penia (67% of pts), Grade 3 or 4 neu- cough, dizziness, fainting, fever, shortness
tropenia (27% and 11% of pts), throm- of breath, weakness, or burning with uri-
bocytopenia (42% of pts), Grade 3 or 4 nation. • Avoid crowds, those with active
thrombocytopenia (5% and 1% of pts), infection. • Take within 1 hr of breakfast
febrile neutropenia (3.8% of pts) may and evening meal. • Drink plenty of flu-
occur. Infectious processes including ids. • Report diarrhea, nausea, vomiting
nasopharyngitis, urinary tract infection that is not controlled by antinausea, an-
reported in 2%–4% of pts. Pulmonary tidiarrheal medication. • Report bleed-
embolism occurred in 2% of pts. Intersti- ing of any kind.
tial lung disease occurs rarely.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT
tisagenlecleucel
Obtain baseline CBC and screen for tis-a-jen-lek-loo-sel
anemia, neutropenia, thrombocytope- (Kymriah)
nia. Obtain vital signs. Verify pregnancy
status before start of each cycle. Screen
j BLACK BOX ALERT jLife-
threatening cytokine release syn-
for active infection, history of pulmonary drome (CRS) was reported. Do not
T administer in pts with inflammatory
embolism. Assess hydration status. Ques-
tion pt’s usual stool characteristics (color, disorders or severe active infection.
frequency, consistency). Treat CRS with tocilizumab and
corticosteroids. Life-threatening
INTERVENTION/EVALUATION neurologic toxicities may occur.
Monitor for neurological events
Follow proper handling and disposal after treatment.
procedures for cytotoxic drugs. Monitor Do not confuse tisagenlecleucel
ANC, CBC on day 15 of each cycle. If any with sipuleucel-T or Kymriah
Grade 3 or 4 hematologic toxicity oc- with Kynamro.
curs, repeat ANC, CBC more frequently.
If chest pain, dyspnea, tachycardia oc- uCLASSIFICATION
curs, provide supplemental O2 and ob- PHARMACOTHERAPEUTIC: Anti-
tain radiologic testing to rule out pul- CD19. Chimeric antigen receptor
monary embolism. Diligently monitor (CAR) T-cell immunotherapy. CLINI-
for infection. Monitor daily stool pat- CAL: Antineoplastic.
tern, consistency. Encourage PO intake.
underlined – top prescribed drug
tisagenlecleucel 1149

USES and antitumor activity). Therapeutic Ef-


Treatment of B-cell precursor acute lym- fect: Causes antitumor activity by initiat-
phoblastic leukemia (ALL) that is refrac- ing activation of T cells.
tory or in second or later relapse in pts up
PHARMACOKINETICS
to 25 yrs of age. Treatment of adults with
relapsed or refractory large B-cell lym- Highly distributed into bone marrow.
phoma after two or more lines of systemic Peak plasma concentration: approx. 10
therapy including diffuse large B-cell lym- days. Half-life: 17 days (ALL); 45 days
phoma (DLBCL) not otherwise specified, (DCBC).
high-grade B-cell lymphoma and DLBCL
LIFESPAN CONSIDERATIONS
arising from follicular lymphoma. Limita-
tions: Not indicated for treatment of pri- Pregnancy/Lactation: May cause fe-
mary central nervous system lymphoma. tal harm due to fetal B-cell depletion and
neonatal lymphocytopenia. Unknown if
PRECAUTIONS distributed in breast milk. Children: Safety
Contraindications: Hypersensitivity to and efficacy has been established. El-
tisagenlecleucel. Cautions: Electrolyte derly: Safety and efficacy not established.
imbalance, elderly pts, renal impairment,
INTERACTIONS
pulmonary disease, cardiac disease;
baseline anemia, neutropenia, leukope- DRUG: Systemic corticosteroids
nia, lymphopenia, thrombocytopenia; (e.g., dexamethasone, prednisone)
conditions predisposing to infection may decrease therapeutic effect; may
(e.g., diabetes, renal failure, immuno- increase risk of infection. May decrease
compromised pts, open wounds); his- therapeutic effect of vaccines. May
tory of venous thromboembolism (DVT, increase adverse/toxic effects of live
PE); pts at risk for acute thrombosis vaccines. Granulocyte colony-stim-
(immobility, indwelling venous catheter/ ulating factors, sargramostim may
access device, morbid obesity, underlying increase adverse/toxic effects of tisa-
atherosclerosis, genetic hypercoagulable genlecleucel. HERBAL: None significant.
conditions); history of HIV infection, FOOD: None known. LAB VALUES: May
hepatitis B or C virus infection; pts at risk increase serum ALT, AST, bilirubin. May
for tumor lysis syndrome (high tumor decrease serum potassium, phosphorus,
burden). Not recommended during ac- sodium; B-cell counts, fibrinogen, immu-
tive infection or in pts with inflammatory noglobulin concentrations, leukocytes,
disorders. Avoid administration of live lymphocytes, neutrophils, platelets. May
vaccines during treatment and after dis- prolong aPTT. T
continuation until B cells are no longer
AVAILABILITY (Rx)
depleted.
Patient-Specific Autologous Infu-
ACTION sion: 0.2–5 × 106 CAR-positive viable
A CD-19–directed genetically modified T cells/kg, 0.1–2.5 × 108 CAR-positive
autologous T-cell immunotherapy that viable T cells, 0.6–6 × 108 CAR-positive
reprograms T cells with a transgene viable T cells.
encoding a chimeric antigen receptor,
ADMINISTRATION/HANDLING
which identifies and eliminates CD19-ex-
pressing malignant and normal cells. CAR b ALERT c Premedicate with acet-
recognizes CD19 and is fused to CD137 aminophen and diphenhydramine (or
(enhances expansion and persistence of another H1 antihistamine) approx. 30–
tisagenlecleucel) and CD3 zeta (a critical 60 min before infusion. Do not use a
component for initiating T-cell activation leukocyte-depleting filter during infu-

Canadian trade name Non-Crushable Drug High Alert drug


1150 tisagenlecleucel
sion. Infusion bags contain human cells bags that have reached room tempera-
genetically modified with a lentivirus. ture must be infused within 30
Follow biosafety handling and safety min. • Do not store thawed infusion
guidelines. bags at 37°C.
IV INDICATIONS/ROUTES/DOSAGE
Preparation • Verify the number of Note: Single-dose infusion(s) contains
infusion bags needed for dose (up to specimen of chimeric antigen receptor
3 cryopreserved patient-specific infu- (CAR)–positive viable T cells. Dose is
sion bags may be required to complete based on weight at the time of leukapher-
a single dose). • Verify dose with esis.
Certificate of Conformance (CoC) and
Certificate of Analysis (CoA). • Thaw- ALL (Relapsed/Refractory)
ing time must be coordinated with infu- Note: Give 2–14 days following lym-
sion time. If more than 1 bag is needed phodepleting chemotherapy with fludara-
for dose, recommend thawing 1 bag at bine and cyclophosphamide.
a time (allows verification that the pre- IV: ADULTS YOUNGER THAN 25 YRS, CHIL-
vious bag was administered safely). • DREN WEIGHING 50 KG OR LESS: 0.2–5
Match pt identity with infusion bag iden- × 106 CAR-positive viable T cells/kg.
tifiers. • Visually inspect for cracks or WEIGHING 50 KG OR MORE: 0.1–2.5 × 108
breaks. Do not infuse if cracks or breaks CAR-positive viable T cells.
are present. • Prime infusion tubing
with 0.9% NaCl. • Thawing: Place DLBCL (Relapsed/Refractory)
infusion bag inside a second sterile Note: Give 2–11 days following lym-
bag to safeguard infusion bag from phodepleting chemotherapy with fludara-
leaks and to protect ports from con- bine and cyclophosphamide.
tamination. • Thaw 1 bag at a time IV: ADULTS: 0.6–6 × 108 CAR-positive
using either a water bath at 37°C or viable T cells.
dry thawing method. • Continue to
thaw until no ice is visible on infusion Dosage in Renal /Hepatic Impairment
bag. Then remove bag from thawing Not specified; use caution.
device. • Visually inspect for clumps.
Gently mix if clumps are present (small SIDE EFFECTS
clumps should disperse). • Do not Frequent (40%–18%): Pyrexia, decreased
infuse if bag is leaking, damaged, or appetite, headache, migraine, tachycar-
T if clumps do not disperse after gentle dia, nausea, diarrhea, vomiting, fatigue,
mixing. • Do not spin down, wash, or malaise, cough, edema (generalized,
resuspend contents. peripheral), delirium, agitation, hal-
Rate of administration • Infuse at lucination, irritability, restlessness, gen-
10–20 mL/min (adjust as needed for eralized pain, constipation. Occasional
small children who require smaller vol- (16%–6%): Abdominal pain, rash (macu-
umes) until all contents are in- lopapular, papular, pruritic), myalgia,
fused. • Upon completion, rinse infu- arthralgia, anxiety, tachypnea, chills, fluid
sion bag with 10–30 mL of 0.9% NaCl overload, back pain, sleep disorder, in-
(while maintaining a closed system) to somnia, nightmares, nasal congestion,
ensure that as many cells as possible are tremor, dizziness, oropharyngeal pain.
administered. Rare (3%–1%): Speech disorder (dysar-
Storage • Infusion bags are frozen thria, aphasia), visual impairment, motor
until time of use. • Thawed infusion dysfunction, muscle spasm.

underlined – top prescribed drug


tisagenlecleucel 1151

ADVERSE EFFECTS/TOXIC NURSING CONSIDERATIONS


REACTIONS
Anemia, leukopenia, lymphopenia, neu- BASELINE ASSESSMENT
tropenia, thrombocytopenia are expected Obtain CBC, BMP, LFT, vital signs; preg-
responses to therapy, but more severe nancy test in females of reproductive
reactions including bone marrow de- potential. Test all pts for hepatitis B or C
pression, febrile neutropenia may be virus infection, HIV infection before cell
life-threatening. Prolonged cytopenias collection. Withhold infusion if any of the
may occur for several wks following lym- following are present: active graft-versus-
phodepleting chemotherapy. Life-threat- host disease, unresolved adverse effect
ening CRS reported in up to 79% of pts. from previous chemotherapies (e.g., car-
Symptoms of CRS may include asthenia, diac reactions, hypotension, pulmonary
hypotension, nausea, pyrexia; elevated reactions); severe, uncontrolled infection;
ALT/AST, bilirubin; disseminated intravas- worsening of leukemia burden following
cular coagulation (DIC), capillary leak lymphodepleting chemotherapy. Ensure
syndrome, hemophagocytic lymphohistio- that tocilizumab, emergency resuscitative
cytosis/macrophage activation syndrome equipment are readily available before
(HLH/MAS). Median time to onset of CRS initiation and following completion. Ques-
was 3–10 days. Infusion reactions may tion history of cardiac disease, pulmonary
be clinically indistinguishable from CRS. disease, chronic infections, renal impair-
Life-threatening neurological toxicities ment, thrombosis. Question for recent
including altered mental status, balance administration of vaccines, live vaccines.
disorders, confusion, disorientation, en- Offer emotional support.
cephalopathy, seizures, speech disorders,
syncope occurred in up to 72% of pts. INTERVENTION/EVALUATION
Median time to onset of neurological tox- Monitor ANC, CBC, BMP, LFT, vital signs
icities was 6–14 days. Cardiac events in- as clinically indicated; immunoglobulin
cluding cardiac failure, cardiac arrest may levels after treatment (and in newborns
occur, esp. in pts with history of cardiac of treated mothers). Manage hypogam-
disease. Life-threatening opportunistic in- maglobulinemia as clinically appropri-
fections, bacterial/viral/fungal infections, ate. Obtain serum calcium, phosphate,
sepsis were reported. Other life-threaten- uric acid if tumor lysis syndrome is sus-
ing or fatal events may include abdominal pected (presents as acute renal failure,
compartment syndrome, acute kidney in- electrolyte imbalance, cardiac arrhyth-
jury, ARDS, graft-versus-host disease, mul- mias, seizures). Diligently monitor for
tiple organ dysfunction syndrome, respira- T
CRS. Recommend observation 2–3 times/
tory distress/failure, seizures, thrombosis wk during the first wk at a health care fa-
(DVT, PE, venous thrombosis). May cause cility. Follow manufacturer’s guidelines
HBV reactivation, resulting in fulminant regarding management of CRS (e.g.,
hepatitis, hepatic failure, or death. Tumor administration of IV fluids, vasopressors,
lysis syndrome may present as acute renal tocilizumab). Monitor for infections of
failure, hypocalcemia, hyperuricemia, any kind. Due to risk of cardiovascular
hyperphosphatemia. Hypogammaglobu- events, have emergency resuscitation
linemia, agammaglobulinemia (IgG) (re- equipment readily available. Conduct
lated to B-cell aplasia) reported in 43% of routine neurological assessments. Moni-
pts. May increase risk of new malignan- tor for symptoms of DVT (leg or arm
cies. Hypersensitivity reactions including pain/swelling), PE (chest pain, dyspnea,
anaphylaxis may occur. Immunogenicity tachycardia). Monitor for bleeding
(anti-mCAR19 antibodies) occurred in events, renal toxicity (anuria, hyperten-
5% of pts. sion, generalized edema, flank pain),

Canadian trade name Non-Crushable Drug High Alert drug


1152 tiZANidine
secondary malignancies, recurrence allergic reactions such as difficulty breath-
of cancer, HBV reactivation (amber to ing, hives, low blood pressure, rash, swell-
orange-colored urine, fatigue, jaundice, ing of the face or tongue. • Treatment
nausea, vomiting), neurological toxici- may cause reactivation of chronic viral in-
ties. Monitor weight, I&Os; daily pattern fections, new cancers.
of bowel activity, stool consistency. En-
sure adequate hydration, nutrition.
PATIENT/FAMILY TEACHING tiZANidine
• Treatment may depress your immune
system and reduce your ability to fight in- tye-zan-i-deen
fection. Report symptoms of infection such (Zanaflex)
as body aches, burning with urination, Do not confuse tiZANidine with
chills, cough, fatigue, fever. Avoid those tiaGABine.
with active infection. • Report symptoms
of bone marrow depression such as bruis- uCLASSIFICATION
ing, fatigue, fever, shortness of breath, PHARMACOTHERAPEUTIC: Alpha 2-
weight loss, bleeding easily, bloody urine adrenergic agonist. CLINICAL: Anti-
or stool. • CRS, a life-threatening condi- spastic.
tion caused by immune activation, may
occur; report difficulty breathing, head-
ache, fever, low blood pressure, rash, USES
rapid heart rate. Stay within the proximity Acute and intermittent management of
of a health care facility for at least 4 wks muscle spasticity (spasms, stiffness, ri-
after infusion. • Therapy may cause tu- gidity), spasticity associated with multiple
mor lysis syndrome (a condition caused sclerosis or spinal cord injury.
by the rapid breakdown of cancer cells),
which can cause kidney failure and can be PRECAUTIONS
fatal. Report decreased urination, amber- Contraindications: Hypersensitivity to
colored urine, confusion, difficulty breath- tiZANidine. Concurrent use with strong
ing, fatigue, fever, muscle or joint pain, CYP1A2 inhibitors (e.g., ciprofloxacin,
palpitations, seizures, vomiting. • Effec- fluvoxamine). Cautions: Renal/hepatic
tive contraception may be required based disease, pts at risk for severe hypotensive
on treatment with other medica- effects, cardiac disease, psychiatric dis-
tions. • Report cardiovascular events orders, elderly pts.
T (e.g., difficulty breathing, fainting, irregu-
lar heartbeats, palpitations, sweat- ACTION
ing). • Report bleeding of any Increases presynaptic inhibition of spi-
kind. • If applicable, vaccinations nal motor neurons mediated by alpha2-
should be up-to-date at least 6 wks before adrenergic agonists, reducing facilita-
starting treatment. Do not receive live vac- tion to postsynaptic motor neurons.
cines. • Report symptoms of DVT (e.g., Therapeutic Effect: Reduces muscle
swelling, pain, hot feeling in the arms or spasticity.
legs; discoloration of extremity), lung em-
bolism (e.g., difficulty breathing, chest PHARMACOKINETICS
pain, rapid heart rate). • Report liver Metabolized in liver. Primarily excreted
problems such as bruising, confusion, in urine. Half-life: 2 hrs.
dark or amber-colored urine, right upper
abdominal pain, or yellowing of the skin INTERACTIONS
or eyes; kidney problems such as de- DRUG: Alcohol, other CNS depres-
creased urine output, dark-colored urine; sants (e.g., LORazepam, ­morphine,
underlined – top prescribed drug
tobramycin 1153
zolpidem) may increase CNS depres- SIDE EFFECTS
sant effects. Strong CYP1A2 inhibi- Frequent (49%–41%): Dry mouth,
tors (e.g., ciprofloxacin, fluvox- drowsiness, asthenia. Occasional (16%–
aMINE) may increase concentration/ 4%): Dizziness, UTI, constipation. Rare
adverse effects (contraindicated). (3%): Nervousness, amblyopia, pharyngi-
HERBAL: Herbals with hypotensive tis, rhinitis, vomiting, urinary frequency.
properties (e.g., garlic, ginger,
ginkgo biloba) may alter effects. ADVERSE EFFECTS/TOXIC
Herbals with sedative properties REACTIONS
(e.g., chamomile, kava kava, va- Hypotension may be associated with
lerian) may increase CNS depression. bradycardia, orthostatic hypotension,
FOOD: None known. LAB VALUES: May and, rarely, syncope. Risk of hypotension
increase serum alkaline phosphatase, increases as dosage increases; hypoten-
ALT, AST. sion is noted within 1 hr after administra-
tion. May cause visual hallucinations.
AVAILABILITY (Rx)
Capsules: 2 mg, 4 mg, 6 mg. Tablets: 2 NURSING CONSIDERATIONS
mg, 4 mg. BASELINE ASSESSMENT

ADMINISTRATION/HANDLING Record onset, type, location, duration of


muscular spasm. Check for immobility,
PO
stiffness, swelling. Obtain LFT.
• Capsules may be opened and sprin-
kled on food. • May give without re- INTERVENTION/EVALUATION
gard to food. • Administration should Assist with ambulation at all times. For
be consistent and not switched between those on long-term therapy, serum he-
giving with or without food. patic/renal function tests should be per-
formed periodically. Evaluate for thera-
INDICATIONS/ROUTES/DOSAGE peutic response (decreased intensity of
Muscle spasticity skeletal muscle pain/tenderness, im-
PO: ADULTS, ELDERLY: Initially, 2 mg proved mobility, decrease in spasticity).
once daily at bedtime. May increase by Go from lying to standing slowly.
2–4 mg at intervals of 1–4 days. Maxi-
PATIENT/FAMILY TEACHING
mum: 36 mg/day in 3–4 divided doses.
Discontinuation of therapy: Gradu- • Avoid tasks that require alertness, mo-
ally taper dose by 2–4 mg daily. tor skills until response to drug is estab-
lished. • Avoid sudden changes in pos- T
Dosage in Renal Impairment ture. • May cause hypotension, sedation,
May require dose reduction/less fre- impaired coordination. • Avoid alcohol.
quent dosing. CrCl less than 25 mL/
min: Reduce dose by 50%. If higher
doses needed, increase dose instead of tobramycin
frequency.
toe-bra-mye-sin
Dosage in Hepatic Impairment (TOBI, Tobrex)
Avoid use if possible. If used, monitor for j BLACK BOX ALERT j May
adverse effects (e.g., hypotension). cause neurotoxicity, nephrotoxic-
ity, ototoxicity. Ototoxicity usually
is irreversible. Increased risk of
neuromuscular blockade, including
respiratory paralysis, particularly

Canadian trade name Non-Crushable Drug High Alert drug


1154 tobramycin
when given after anesthesia or mus- brain barrier; low concentrations in CSF).
cle relaxants. May cause fetal harm. Excreted unchanged in urine. Removed by
Do not confuse tobramycin with hemodialysis. Half-life: 2–4 hrs (increased
vancomycin, or Tobrex with in renal impairment, neonates; decreased in
TobraDex. cystic fibrosis, febrile or burn pts).
FIXED-COMBINATION(S) LIFESPAN CONSIDERATIONS
TobraDex: tobramycin/dexametha- Pregnancy/Lactation: Drug readily
sone (a steroid): 0.3%/0.1% per mL crosses placenta; distributed in breast
or per g. Zylet: tobramycin/lotepred- milk. May cause fetal nephrotoxicity.
nol: 0.3%/0.5%. Ophthalmic form should not be used in
uCLASSIFICATION breastfeeding mothers and only when
specifically indicated in pregnancy.
PHARMACOTHERAPEUTIC: Amino- Children: Immature renal function
glycoside. CLINICAL: Antibiotic. in neonates, premature infants may
increase risk of toxicity. Elderly: Age-
USES related renal impairment may increase
risk of toxicity; dosage adjustment rec-
Treatment of susceptible infections due ommended.
to P. aeruginosa, other gram-negative
organisms including skin/skin structure, INTERACTIONS
bone, joint, respiratory tract infections;
DRUG: May decrease therapeutic ef-
postop, burn, intra-abdominal infections;
fect of BCG (intravesical), vaccine
complicated UTI; septicemia; meningitis.
(live). Foscarnet, mannitol may
Ophthalmic: Superficial eye infections:
increase nephrotoxic effect. Penicil-
blepharitis, conjunctivitis, keratitis, cor-
lin may decrease concentration/effect.
neal ulcers. Inhalation: Bronchopul-
HERBAL: None significant. FOOD: None
monary infections (Pseudomonas aeru-
known. LAB VALUES: May increase
ginosa) in pts with cystic fibrosis.
serum BUN, bilirubin, creatinine, alka-
PRECAUTIONS line phosphatase, LDH, ALT, AST. May
decrease serum calcium, magnesium,
Contraindications: Hypersensitivity to
potassium, sodium. Therapeutic peak
tobramycin, other aminoglycosides
serum level: 5–20 mcg/mL; therapeu-
(cross-sensitivity) and their components.
tic trough serum level: 0.5–2 mcg/mL.
Cautions: Renal impairment, preexist-
Toxic peak serum level: greater than
T ing au­di­tory or vestibular impairment,
20 mcg/mL; toxic trough serum level:
conditions that depress neuromuscular
greater than 2 mcg/mL.
transmission, Parkinson’s disease, myas-
thenia gravis, hypocalcemia, pregnancy, AVAILABILITY (Rx)
elderly pts.
Infusion, Premix: 60 mg/50 mL, 80
ACTION mg/100 mL. Inhalation Powder: (TOBI
Podhaler): 28 mg in a capsule. Injection,
Irreversibly binds to protein on bacterial Powder for Reconstitution: 1.2 g. Injec-
ribosomes. Therapeutic Effect: Inter- tion Solution: 10 mg/mL, 40 mg/mL.
feres with protein synthesis of susceptible Ointment, Ophthalmic: (Tobrex): 0.3%.
microorganisms. Solution, Nebulization: (TOBI): 60 mg/
mL. Solution, Ophthalmic: (Tobrex): 0.3%.
PHARMACOKINETICS
Rapid, complete absorption after IM admin- ADMINISTRATION/HANDLING
istration. Protein binding: less than 30%. b ALERT c Coordinate peak and trough
Widely distributed (does not cross blood- lab draws with administration times.
underlined – top prescribed drug
tobramycin 1155

IV IV COMPATIBILITIES
Amiodarone (Cordarone), calcium gluco-
Reconstitution • Dilute with 50–100 nate, cefepime, ceftaroline, cefTAZidime,
mL D5W or 0.9% NaCl. Amount of diluent dexmedetomidine (Precedex), dilTIAZem
for infants, children depends on individ- (Cardizem), furosemide (Lasix), HYDRO-
ual need. morphone (Dilaudid), insulin, linezolid
Rate of administration • Infuse over (Zyvox), magnesium sulfate, midazolam
30–60 min. (Versed), morphine, niCARdipine
Storage • Store vials at room temper- (Cardene), tigecycline (Tygacil).
ature. • Solutions may be discolored by
light or air (does not affect po- INDICATIONS/ROUTES/DOSAGE
tency). • Reconstituted solution stable b ALERT c Space parenteral doses
for 24 hrs at room temperature or 96 hrs evenly around the clock. Dosage based
if refrigerated. on ideal body weight. Peak, trough levels
IM
determined periodically to maintain de-
• To minimize discomfort, give deep IM sired serum concentrations (minimizes
slowly. • Less painful if injected into risk of toxicity). Recommended peak
gluteus maximus rather than lateral as- level: 4–10 mcg/mL; trough level: 0.5–2
pect of thigh. mcg/mL.
Usual Parenteral Dosage
Inhalation
IV: ADULTS, ELDERLY: 3–7.5 mg/kg/day in
• Refrigerate. • May store at room
temperature up to 28 days after removing 3 divided doses. Once-daily dosing: 4–7
from refrigerator. • Do not use if cloudy mg/kg every 24 hrs. CHILDREN 5 YRS AND
OLDER: 2–2.5 mg/kg/dose q8h. CHILDREN
or contains particulates. • Podhaler:
YOUNGER THAN 5 YRS: 2.5 mg/kg/dose
Pt must not swallow capsules. • Doses
should be as close as possible to 12 hrs q8h. NEONATES LESS THAN 1 KG (14 DAYS
OR YOUNGER): 5 mg/kg/dose q48h; (15–28
apart and not less than 6 hrs apart. • Use
DAYS): 5 mg/kg/dose q36h. 1–2 KG (7 DAYS
Podhaler device supplied.
OR YOUNGER): 5 mg/kg/dose q48h; (8–28
Ophthalmic DAYS): 5 mg/kg/dose q36h. GREATER THAN
• Place gloved finger on lower eyelid, 2 KG (7 DAYS OR YOUNGER): 4 mg/kg q24h;
pull out until pocket is formed between (8–28 DAYS): 4–5 mg/kg q24h.
eye and lower lid. • Place correct num-
Usual Ophthalmic Dosage
ber of drops (14–12 inch ointment) into
pocket. • Solution: Apply digital pres- Ophthalmic ointment: ADULTS, EL- T
sure to lacrimal sac for 1–2 min (mini- DERLY, CHILDREN 2 MOS AND OLDER:Apply
mizes drainage into nose/throat, reducing 12 inch to conjunctiva q8–12h (q3–4h
risk of systemic effects). • Ointment: for severe infections).
Ophthalmic solution: ADULTS, EL-
Instruct pt to close eye for 1–2 min, roll-
ing eyeball (increases contact area of DERLY, CHILDREN 2 MOS AND OLDER: 1–2
drug to eye). • Remove excess solution/ drops in affected eye q4h (2 drops/hr for
ointment around eye. severe infections).
Usual Inhalation Dosage (Cystic Fibrosis)
IV INCOMPATIBILITIES
Inhalation high dose: ADULTS, CHIL-
Amphotericin B complex (Abelcet, DREN 6 YRS AND OLDER: 300 mg q12h
AmBisome, Amphotec), heparin, indo- 28 days on, 28 days off. (Tobi Pod-
methacin (Indocin), piperacillin-tazo- haler): Four 28-mg capsules twice
bactam (Zosyn), propofol (Diprivan), daily for 28 days followed by 28 days
sargramostim (Leukine, Prokine). off.

Canadian trade name Non-Crushable Drug High Alert drug


1156 tocilizumab
Dosage in Renal Impairment sides, sulfite (and parabens for topical,
Dosage and frequency modified based on ophthalmic routes). Establish baseline
degree of renal impairment, serum drug hearing acuity. Obtain baseline lab tests,
concentration. After loading dose of 1–2 esp. renal function.
mg/kg, maintenance dose and frequency
INTERVENTION/EVALUATION
are based on serum creatinine levels,
creatinine clearance. Monitor I&O (maintain hydration), uri-
Creatinine Clearance Dosing Interval nalysis, renal function. Monitor results
41–60 mL/min q12h
of peak/trough blood tests. Thera-
21–40 mL/min q24h peutic serum level: peak: 5–20 mcg/
10–20 mL/min q48h mL; trough: 0.5–2 mcg/mL. Toxic se-
Less than 10 mL/min q72h rum level: peak: greater than 20 mcg/
Hemodialysis Loading dose 2–3 mL; trough: greater than 2 mcg/mL. Be
mg/kg then 1–2 alert to ototoxic, neurotoxic symptoms.
mg/kg q48–72h Evaluate IV site for phlebitis (heat, pain,
Continuous renal Loading dose 2–3 red streaking over vein). Assess for rash.
­replacement mg/kg then 1–2.5
­therapy mg/kg q24–48h
Be alert for superinfection, particularly
anal/genital pruritus, changes of oral
mucosa, diarrhea. When treating pts
Dosage in Hepatic Impairment with neuromuscular disorders, assess
No dose adjustment. respiratory response carefully. Oph-
thalmic: Assess for redness, swelling,
SIDE EFFECTS itching, tearing.
Occasional: IM: Pain, induration.
PATIENT/FAMILY TEACHING
IV: Phlebitis, thrombophlebitis. Topi-
cal: Hypersensitivity reaction (fever, • Report any hearing, visual, balance,
pruritus, rash, urticaria). Ophthalmic: urinary problems, even after therapy is
Tearing, itching, redness, eyelid swelling. completed. • Ophthalmic: Blurred vi-
Rare: Hypotension, nausea, vomiting. sion, tearing may occur briefly after ap-
plication. • Report persistent tearing,
ADVERSE EFFECTS/TOXIC redness, irritation.
REACTIONS
Nephrotoxicity (acute kidney injury, acute
tubular necrosis, renal failure) may be
reversible if drug is stopped at first sign tocilizumab
T of symptoms. Irreversible ototoxicity (diz-
ziness, ringing/roaring in ears, hearing toe-si-liz-oo-mab
loss), neurotoxicity (headache, dizziness, (Actemra)
lethargy, tremor, visual disturbances) oc- j BLACK BOX ALERT jTuber-
cur occasionally. Risk increases with higher culosis, serious invasive fungal
infections, other opportunistic
dosages or prolonged therapy or if solution infections have occurred. Test for
is applied directly to mucosa. Superinfec- tuberculosis prior to and during
tions, particularly fungal infections, may treatment, regardless of initial
result from bacterial imbalance with any ad- result. Consider treatment of latent
ministration route. Anaphylaxis may occur. TB prior to initiation.

NURSING CONSIDERATIONS uCLASSIFICATION

BASELINE ASSESSMENT
PHARMACOTHERAPEUTIC: Inter-
leukin (IL)-6 receptor inhibitor.
Dehydration must be treated before be- CLINICAL: Antirheumatic, disease-
ginning parenteral therapy. Question for modifying agent.
history of allergies, esp. aminoglyco-
underlined – top prescribed drug
tocilizumab 1157

USES INTERACTIONS
Treatment of moderate to severe rheuma- DRUG: May increase adverse effects of
toid arthritis in adults who had inadequate abatacept, belimumab, natalizumab,
response to disease-modifying antirheu- tofacitinib, vaccines (live). May de-
matic drugs (DMARDs). Treatment of crease therapeutic effect of vaccines
active systemic juvenile idiopathic arthri- (live). Baricitinib may increase adverse
tis (SJIA) in pts 2 yrs of age and older. effects. May increase immunosuppressive
Treatment of active polyarticular juvenile effect of anti-TNF agents (e.g., adali-
idiopathic arthritis (PJIA) in pts 2 yrs and mumab, etanercept, infliximab).
older. Treatment of adults and children 2 HERBAL: Echinacea may alter levels/
yrs of age and older with chimeric antigen effects. FOOD: None known. LAB VAL-
receptor (CAR) T cell–induced severe or UES: May increase serum ALT, AST, lip-
life-threatening cytokine release syndrome. ids. May decrease platelets, neutrophils.
Treatment of giant cell arteritis in adults.
AVAILABILITY (Rx)
PRECAUTIONS Injection Solution:20 mg/mL (80 mg/4
Contraindications: Hypersensitivity to mL, 200 mg/10 mL, 400 mg/20 mL). Sy-
ringe for SQ Administration: 162 mg/0.9
tocilizumab. Cautions: Platelet count
100,000 cells/mm3 or less, ANC less than mL. Syringe Auto-injector: 162 mg/0.9
2,000 cells/mm3, ALT, AST greater than mL.
1.5 times upper limit of normal (ULN) ADMINISTRATION/HANDLING
prior to treatment. Do not administer b ALERT c Do not infuse IV push or
to pts with active infection. Preexisting bolus.
or recent-onset CNS demyelinating dis-
orders, including multiple sclerosis; pts IV
with chronic or recurrent infection or
who have been exposed to tuberculosis; Reconstitution • Dilute in 100 mL
hematologic cytopenia, hepatic impair- 0.9% NaCl (50 mL 0.9% NaCl for SJIA pts
ment, elderly pts, pts at increased risk weighing less than 30 kg). • Prior to
of GI perforation. Avoid live vaccinations. mixing, withdraw and discard volume of
NaCl equal to volume of patient-dosed
ACTION solution. • Invert bag to avoid foam-
ing. • Inject solution and dilute for
Binds to IL-6 receptors, inhibiting signals mixture that equals 50 mL or 100 mL in
of proinflammatory cytokines. Thera- NaCl bag.
peutic Effect: Inhibits/slows structural Rate of administration • Infuse over T
joint damage, improves physical function. 1 hr.
Storage • Refrigerate vials; do not
PHARMACOKINETICS freeze. • Diluted solutions may be
Distributed in steady state of plasma and stored for 24 hrs at room temperature or
tissue compartments. Undergoes bipha- refrigerated. • Protect from light until
sic elimination from circulation. Half- time of use. • Solution appears color-
life: 11–13 days. less. Discard solution if it appears cloudy,
discolored, or contains particulate.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown INDICATIONS/ROUTES/DOSAGE
if distributed in breast milk. Chil- Note: Do not infuse concomitantly in
dren: Safety and efficacy not estab- same IV line with other drugs. Do not
lished in conditions other than SJIA. begin if ANC less than 2,000 cells/mm3,
Elderly: Cautious use due to increased platelets less than 100,000 cells/mm3, or
risk of serious infections, malignancy. ALT or AST more than 1.5 times ULN.
Canadian trade name Non-Crushable Drug High Alert drug
1158 tocilizumab
Moderate to Severely Active Rheumatoid SQ: WEIGHING 30 KG OR GREATER: 162 mg
Arthritis q2wks. WEIGHING LESS THAN 30 KG: 162
IV: ADULTS, ELDERLY: 4 mg/kg every 4 mg q3wks.
wks initially. May increase to 8 mg/kg ev-
ery 4 wks. Maximum: 800 mg per dose. Dosage in Renal Impairment
SQ: ADULTS, ELDERLY WEIGHING 100 KG OR Mild impairment: No dose adjust-
GREATER: 162 mg/wk. WEIGHING LESS THAN ment. Moderate to severe impair-
100 KG: 162 mg every other wk. May increase ment: Use caution (not studied).
to every wk based on clinical response.
Dosage in Hepatic Impairment
Cytokine Release Syndrome Not recommended.
IV: ADULTS, CHILDREN WEIGHING 30 KG
OR GREATER: 8 mg/kg. PTS WEIGHING SIDE EFFECTS
LESS THAN 30 KG: 12 mg/kg. If no clini- Occasional (8%–6%): Upper respiratory
cal improvement, 3 additional doses may tract infection, nasopharyngitis, head-
be given with an interval of at least 8 hrs. ache, hypertension. Rare (5%–3%): Infu-
Maximum: 800 mg/dose. sion reaction, dizziness, bronchitis, rash,
oral ulceration.
Giant Cell Arteritis
SQ: ADULTS, ELDERLY: 162 mg once every ADVERSE EFFECTS/TOXIC
wk (in combination with tapering course REACTIONS
of glucocorticoid). May be given alone fol- Up to 48% of pts experience elevated
lowing discontinuation of glucocorticoid. ALT, AST. Neutropenia, thrombocytopenia
Dosage Modification occur in 4% of pts. Serious infections,
Hepatic enzyme levels greater than ULN. including sepsis, pneumonia, tuberculo-
Lab Value Recommendation sis, invasive fungal infections, hepatitis
1–3 times Dose modify concomitant B, have occurred. Anaphylactic reaction,
ULN DMARDs or reduce rash, pruritus, urticaria, bronchospasm,
dose to 4 mg/kg until swelling, dyspnea occur in less than
ALT, AST normalized 0.2% of pts; hypersensitivity reactions
Greater than Interrupt treatment until (hypertension, headaches, flushing)
3–5 times ALT, AST less than 3 occur more frequently. Increased risk
ULN times ULN, then follow of lymphoma, melanoma. New onset or
guidelines for 1–3 times
ULN
exacerbation of CNS demyelinating disor-
Greater than Discontinue treatment ders, including multiple sclerosis. Risk of
T 5 times ULN gastric perforation with concomitant use
of NSAIDs, corticosteroids.
SJIA
NURSING CONSIDERATIONS
IV: CHILDREN WEIGHING 30 KG OR GRE­
ATER: 8 mg/kg q2wks. CHILDREN WEIGHING BASELINE ASSESSMENT
LESS THAN 30 KG: 12 mg/kg q2wks. Evaluate pt for active tuberculosis and
SQ: CHILDREN WEIGHING 30 KG OR GRE­ test for latent infection prior to initiating
ATER:162 mg once every wk. CHILDREN treatment and periodically during therapy.
WEIGHING LESS THAN 30 KG: 162 mg q2wks. Induration of 5 mm or greater with tuber-
culin skin testing should be considered a
PJIA
positive test result when assessing for latent
IV: CHILDREN WEIGHING 30 KG OR
tuberculosis. Antifungal therapy should be
GREATER: 8 mg/kg q4wks. CHILDREN
considered for pts who reside or travel to
WEIGHING LESS THAN 30 KG: 10 mg/kg
regions where mycoses are endemic. Do
q4wks.
not initiate therapy during an active infec-
tion. Viral reactivation can occur in cases
underlined – top prescribed drug
tofacitinib 1159
of herpes zoster, HIV. Assess baseline lab schedule. • Decreased platelet count
results (hepatic enzymes, cholesterol, may lead to risk of bleeding.
triglycerides, platelets, neutrophils) q4–
8wks during treatment. Pts should report
history of diverticulitis, weakened immune tofacitinib
system, HIV, hepatic disease, GI bleeding,
hemoptysis, diarrhea, weight loss, cancer, toe-fa-sye-ti-nib
prior cancer treatment, use of NSAIDs, (Xeljanz, Xeljanz XR)
glucocorticosteroids. j BLACK BOX ALERT jIncreased
risk for developing bacterial, viral,
INTERVENTION/EVALUATION invasive fungal, other opportunistic
Monitor hepatitis B carriers during and infections including tuberculosis,
cryptococcosis, pneumocystosis
several months following therapy. If re- that may lead to hospitalization or
activation occurs, consider interrupting death; infections often occurred in
treatment. Monitor pts for signs/symptoms combination with other immu-
of tuberculosis regardless of baseline nosuppressants (methotrexate,
PPD. Discontinue treatment if pt develops corticosteroids). Closely monitor
for development of infection. Test
acute infection, opportunistic infection, or for latent tuberculosis prior to
sepsis and initiate appropriate antimicro- treatment and during treatment,
bial therapy. Monitor warfarin, theophyl- regardless of initial result. Treat-
line, cycloSPORINE levels for therapeutic ment for latent TB should be
ranges. Modify, interrupt, or discontinue initiated before use. Malignancies
including lymphoma, nonmelanoma
treatment if ALT, AST is 1–5 times ULN. skin cancer reported. Increased
rate of Epstein-Barr virus–associ-
PATIENT/FAMILY TEACHING
ated post-transplant lymphoprolif-
• Inform pt that therapy may lower im- erative disorder observed in renal
mune system response. • Detail any transplant pts who are treated with
concomitant immunosuppressive ther- tofacitinib and other immunosup-
pressive therapy drugs.
apy, methotrexate. • Report any history
Do not confuse tofacitinib with
of HIV, fungal infections, hepatitis B,
tipifarnib or Xeljanz with Xeloda.
multiple sclerosis, hemoptysis, tubercu-
losis, or close relatives with active tuber- uCLASSIFICATION
culosis. • Report any travel plans to
PHARMACOTHERAPEUTIC: Janus-
possible endemic areas. • Report
associated kinase (JAK) inhibitor.
signs/symptoms of stomach pain to eval-
CLINICAL: Antirheumatic, disease-
uate risk of gastric perforation or history T
modifying.
of taking NSAIDs, corticosteroids, metho-
trexate. • Pt will need blood levels
drawn q4–8wks during treatment along USES
with routine tuberculosis screen- Treatment of adult pts with moderate to se-
ing. • Seek immediate medical atten- vere active rheumatoid arthritis with previous
tion if adverse reaction occurs. • Do inadequate response or intolerance to meth-
not receive live vaccines during ther- otrexate. May be used as monotherapy or
apy. • Notify physician if pregnant or in combination with methotrexate or other
planning on becoming pregnant. • Dur- nonbiologic disease-modifying antirheu-
ing treatment, report any signs of liver matic drugs (DMARDs). Treatment of active
problems, such as stomach pains, yel- psoriatic arthritis (PsA) in pts who have had
lowing of skin/eyes, dark-amber urine, inadequate response to methotrexate, other
clay-colored or bloody stools, fatigue, DMARDs. Treatment of moderate to severe
reduced appetite, coffee-ground eme- active ulcerative colitis (UC) in adults. Do
sis. • Pt must adhere to strict dosing not use in combination with other biologic

Canadian trade name Non-Crushable Drug High Alert drug


1160 tofacitinib
DMARDs or with potent immunosuppres- tration/effect. CYP3A4 inducers (e.g.,
sants (e.g., azaTHIOprine, cycloSPORINE). phenytoin, rifAMPin) may decrease
concentration/effect. May increase adverse
PRECAUTIONS effects; decrease therapeutic effect of vac-
Contraindications: Hypersensitivity to to- cines (live). HERBAL: St. John’s wort
facitinib. Cautions: Pts exposed to TB, his- may decrease concentration/effect. Echi-
tory of serious opportunistic infections, con- nacea may decrease the therapeutic effect.
ditions that predispose to infections (e.g., FOOD: None known. LAB VALUES: May
diabetes), pts at risk for GI perforation (e.g., increase ALT, AST, bilirubin, lipids, creati-
diverticulitis), pts who resided or traveled nine. May decrease Hgb, neutrophils, lym-
in areas where TB is endemic, moderate phocytes.
to severe renal impairment, elderly pts, he-
patic impairment, history of anemia, hyper- AVAILABILITY (Rx)
lipidemia, hepatitis, Asian ancestry, pts with Tablets, Film-Coated: (Xeljanz): 5 mg.
history of interstitial lung disease, heart rate (Xeljanz XR): 11 mg.
less than 60 bpm, conduction abnormali-
ties, ischemic heart disease, HF. ADMINISTRATION/HANDLING
PO
ACTION • Give without regard to food. • Do
Inhibits JAK enzymes, which are intracel- not cut, split, crush, or chew XR tablet.
lular enzymes involved in stimulating he-
matopoiesis and immune cell functioning INDICATIONS/ROUTES/DOSAGE
through a signaling pathway. Therapeutic b ALERT c Do not initiate treatment in
Effect: Reduces inflammation, tenderness, pts with baseline active infection (sys-
swelling of joints; slows or prevents progres- temic/localized), severe hepatic impair-
sive joint destruction in rheumatoid arthritis ment, lymphocytes less than 500 cells/
(RA). Prevents cytokine or growth factor mm3, ANC less than 1,000 cells/mm3,
gene expression, reducing circulating natu- Hgb less than 9 g/dL.
ral killer cells and increasing B cells.
Rheumatoid Arthritis (Monotherapy or
PHARMACOKINETICS with Nonbiologic DMARD)
Rapidly absorbed following PO administra- PO: ADULTS/ELDERLY: (Xeljanz): 5 mg
tion. Protein binding: 40%. Peak concentra- twi­ce daily. (Xeljanz XR): 11 mg once daily.
tion: 30–60 min. Metabolized in liver. Ex-
creted primarily in urine. Half-life: 3 hrs. PsA (with Nonbiologic DMARD)
T PO: ADULTS/ELDERLY: (Xeljanz): 5 mg twi­ce
LIFESPAN CONSIDERATIONS daily. (Xeljanz XR): 11 mg once daily.
Pregnancy/Lactation: Not recom- UC
mended in nursing mothers. Must either PO: ADULTS/ELDERLY: (Xeljanz): Induc-
discontinue drug or discontinue breast- tion: 10 mg twice daily for 8 wks. May
feeding. Unknown if distributed in breast transition to maintenance dose or con-
milk. Children: Safety and efficacy not tinue 10 mg twice daily for additional 8
established. Elderly: Increased risk for wks. Discontinue if 10 mg twice daily is in-
serious infections, malignancy. effective after 4 mos. Maintenance: 5 mg
INTERACTIONS twice daily. May increase to 10 mg twice
daily for shortest duration. Use lowest ef-
DRUG: Immunosuppressants (e.g., fective dose to maintain response.
azaTHIOprine, cycloSPORINE) may
increase risk for added immunosuppres- Dose Modification
sion, infection. CYP3A4 inhibitors (e.g., Reduce to 5 mg once daily for any of the
ketoconazole) may increase concen- following: moderate to severe renal impair-

underlined – top prescribed drug


tofacitinib 1161
ment, moderate hepatic impairment, con- various malignancies. May induce viral re-
current use of potent CYP3A4 inhibitors, activation of hepatitis B or C virus infection,
concurrent use of one or more moderate herpes zoster, HIV. Epstein-Barr virus–as-
CYP3A4 or potent CYP2C19 inhibitors. sociated post-transplant lymphoproliferative
disorder reported in 2% of pts with renal
Lymphopenia transplant. Increased risk for GI perforation.
Interrupt treatment until lymphocytes
greater than or equal to 500 cells/mm3. NURSING CONSIDERATIONS
Discontinue if lymphocytes less than 500
cells/mm3 after repeat testing. BASELINE ASSESSMENT
Obtain vital signs, CBC, BMP, LFT, lipid
Neutropenia panel, urine pregnancy test results. Evalu-
Interrupt treatment until neutrophils ate for active tuberculosis (TB) and test
greater than 1,000 cells/mm3. Discon- for latent infection prior to and during
tinue if neutrophils less than 500 cells/ treatment. Induration of 5 mm or greater
mm3 after repeat testing. with purified protein derivative (PPD) is
Anemia
considered positive result when assessing
Interrupt treatment until Hgb greater for latent TB. Question possibility of preg-
than or equal to 9 g/dL or baseline Hgb nancy or breastfeeding. Screen for history/
decreases less than or equal to 2 g/dL af- co-morbidities. Obtain full medication his-
ter repeat testing. tory including vitamins, herbal products.
INTERVENTION/EVALUATION
Hepatotoxicity
Interrupt treatment until diagnosis of Obtain CBC every 4–8 wks, then every 3
drug-induced hepatic injury has been mos, lipid panel 4–8 wks after initiation; he-
excluded. patic function panel if hepatic ­impairment
suspected. Monitor for TB regardless of
Dosage in Renal Impairment baseline PPD. Consider discontinuation if
Mild impairment: No dose adjust- pt develops acute infection, opportunistic
ment. Moderate to severe impair- infection, sepsis; initiate appropriate anti-
ment: 5 mg once daily. microbial therapy. Immediately report any
hemorrhaging, melena, abdominal pain,
Dosage in Hepatic Impairment hemoptysis (may indicate GI perforation).
Mild impairment: No dose adjustment.
Moderate impairment: 5 mg once daily. PATIENT/FAMILY TEACHING
Severe impairment: Not recommended. • Routinely monitor blood levels. •
Therapy will lower immune system re- T
SIDE EFFECTS sponse. • Do not receive live virus vac-
Rare (4%–2%): Upper respiratory tract cines. • Other immunosuppressant drugs
infection, diarrhea, nasopharyngitis, may increase risk for infection. • Expect
headache, hypertension. routine TB screening. • Fever, cough,
burning with urination, body aches, chills,
ADVERSE EFFECTS/TOXIC skin changes may indicate infection. • Re-
REACTIONS port history of HIV, recent infections, hepa-
Neutropenia, lymphopenia may increase titis B or C, TB or close relatives who have
risk for infection. Serious infections may active TB. • Report any travel plans to
include aspergillosis, BK virus, cellulitis, possible endemic areas. • Notify physi-
coccidioidomycosis, cryptococcus, cy- cian if pregnant or planning preg-
tomegalovirus, esophageal candidiasis, nancy. • Do not breastfeed. • Immedi-
histoplasmosis, invasive fungal infections, ately report bleeding of any kind. •
listeriosis, pneumocystosis, pneumonia, Yellowing of skin or eyes, right upper quad-
tuberculosis, UTI, sepsis. Increased risk for rant abdominal pain, bruising, clay-colored
Canadian trade name Non-Crushable Drug High Alert drug
1162 tolterodine
stool, dark urine may indicate liver prob- LIFESPAN CONSIDERATIONS
lem. • Avoid grapefruit products. Pregnancy/Lactation: Unknown if drug
is distributed in breast milk. Breastfeeding
tolterodine not recommended. Children: Safety and
efficacy not established. Elderly: No
age-related precautions noted.
tol-ter-oh-deen
(Detrol, Detrol LA) INTERACTIONS
Do not confuse Detrol with
Ditropan, or tolterodine with DRUG: Strong CYP3A4 inhibitors
fesoterodine. (e.g., clarithromycin, ketocon-
azole) may increase concentration.
uCLASSIFICATION Strong CYP3A4 inducers (e.g., car-
PHARMACOTHERAPEUTIC: Antimus- BAMazepine, phenytoin, rifAMPin)
carinic agent. CLINICAL: Antispas- may decrease concentration/effect.
modic. Anticholinergics (e.g., aclidinium,
ipratropium, tiotropium, umecli-
dinium) may increase anticholinergic
USES effect. Strong CYP2D6 inhibitors
(e.g., FLUoxetine, PARoxetine) may
Treatment of overactive bladder in pts inhibit drug metabolism. HERBAL: St.
with symptoms of urinary frequency, ur- John’s wort may decrease concentra-
gency, or urge incontinence. tion/effects. FOOD: None known. LAB
PRECAUTIONS VALUES: None known.
Contraindications: Hypersensitivity to tol­ AVAILABILITY (Rx)
terodine or fesoterodine. Gastric retention,
uncontrolled narrow-angle glaucoma, uri- Tablets: (Detrol): 1 mg, 2 mg.
nary retention. Cautions: Renal impair- Capsules, Extended-Release: (Detrol
ment, clinically significant bladder outflow LA): 2 mg, 4 mg.
obstruction (risk of urinary retention),
GI obstructive disorders (e.g., pyloric ste- ADMINISTRATION/HANDLING
nosis [risk of gastric retention]), treated PO
narrow-angle glaucoma, myasthenia gravis, • May give without regard to
prolonged QT interval (congenital/medica- food. • Give extended-release capsules
tions, hypokalemia, hypomagnesemia), he- whole; do not break, crush, or open.
T patic impairment, elderly.
INDICATIONS/ROUTES/DOSAGE
ACTION Overactive Bladder
Antagonist of muscarinic receptors mediat- PO: ADULTS, ELDERLY: (Immediate-
ing urinary bladder contraction. Increases Release): 1–2 mg twice daily (WITH
residual urine volume, reduces detrusor CYP3A4 INHIBITORS): 1 mg twice daily.
muscle pressure. Therapeutic Effect: De- (Extended-Release): 2–4 mg once
creases urinary frequency, urgency. daily. (WITH CYP3A4 INHIBITORS): 2 mg
once daily.
PHARMACOKINETICS
Immediate-release form rapidly, well ab- Dosage in Renal/Hepatic Impairment
sorbed after PO administration. Protein Mild to moderate impairment: (Im-
binding: 96%. Metabolized in liver. Primar- mediate-Release): 1 mg twice daily.
ily excreted in urine. Unknown if removed Use caution. (Extended-Release): 2
by hemodialysis. Half-life: Immediate-re- mg once daily. Use caution. Severe im-
lease: 2–10 hrs. Extended-release: 7–18 hrs. pairment: Not recommended.

underlined – top prescribed drug


topiramate 1163

SIDE EFFECTS USES


Frequent (40%): Dry mouth. Occasional Monotherapy for treatment of partial-
(11%–4%): Headache, dizziness, fatigue, onset or primary generalized tonic-clonic
constipation, dyspepsia, upper respiratory seizures in pts 2 yrs and older (immedi-
tract infection, UTI, dry eyes, abnormal vi- ate-release, Qudexy XR) or 6 yrs and older
sion (accommodation problems), nausea, (Trokendi XR). Adjunctive therapy for
diarrhea. Rare (3%): Drowsiness, chest/back partial-onset, primary generalized tonic-
pain, arthralgia, rash, weight gain, dry skin. clonic seizures or seizures associated with
Lennox-Gastaut syndrome in pts 2 yrs and
ADVERSE EFFECTS/TOXIC older (immediate-release, Qudexy XR) or
REACTIONS 6 yrs and older (Trokendi XR). Prevention
Overdose can result in severe anticholin- of migraine headache in pts 12 yrs and
ergic effects, including abdominal cramps, older. OFF-LABEL: Neuropathic pain, dia-
facial warmth, excessive salivation/lacrima- betic neuropathy, prophylaxis of cluster
tion, diaphoresis, pallor, urinary urgency, headaches, infantile spasms.
blurred vision, prolonged QT interval.
PRECAUTIONS
NURSING CONSIDERATIONS Contraindications: Hypersensitivity to topi-
BASELINE ASSESSMENT ramate. Extended-Release: Trokendi
XR: Recent alcohol use (within 6 hrs
Assess degree of overactive bladder prior to or after). Qudexy XR: Pts with
(urinary urgency, frequency, inconti- metabolic acidosis who are taking met-
nence). Question history as listed in FORMIN. Cautions: Hepatic/renal impair-
Precautions. ment, elderly pts, pts who are at high risk
INTERVENTION/EVALUATION for suicide, respiratory impairment, pts
Assist with ambulation if dizziness oc- with congenital metabolism dysfunction or
curs. Question for visual changes. Moni- decreased mitochondrial activity. During
tor incontinence, postvoid residuals. strenuous exercise, exposure to high en-
vironmental temperature, concomitant use
PATIENT/FAMILY TEACHING of medications with anticholinergic activity.
• May cause blurred vision, dry eyes/
mouth, constipation. • Report any con- ACTION
fusion, altered mental status. • Avoid Blocks neuronal sodium channels, en-
tasks that require alertness, motor skills hances GABA activity; antagonizes glu-
until response to drug is established. tamate receptors and weakly inhibits
carbonic anhydrase. Therapeutic Ef- T
fect: Decreases seizure activity.
topiramate
PHARMACOKINETICS
toe-peer-a-mate Rapidly absorbed after PO administra-
(Qudexy XR, Topamax, Topamax tion. Protein binding: 15%–41%. Me-
Sprinkle, Trokendi XR) tabolized in liver. Primarily excreted
Do not confuse Topamax or unchanged in urine. Removed by hemo-
topiramate with TEGretol, dialysis. Half-life: 21 hrs.
TEGretol XR, or Toprol XL.
LIFESPAN CONSIDERATIONS
uCLASSIFICATION Pregnancy/Lactation: Unknown if
PHARMACOTHERAPEUTIC: Miscel- distributed in breast milk. Children: No
laneous agent. CLINICAL: Anticon- age-related precautions noted in pts older
vulsant. than 2 yrs. Elderly: Age-related renal im-
pairment may require dosage adjustment.
Canadian trade name Non-Crushable Drug High Alert drug
1164 topiramate

INTERACTIONS Initially, 25 mg once or twice daily for


DRUG: Alcohol, other CNS depres- 1 wk. May increase by 25–50 mg/day at
sants (e.g., LORazepam, morphine, wkly intervals. Usual maintenance dose:
zolpidem) may increase CNS depression. 100–200 mg twice daily (partial-onset)
Strong CYP3A4 inducers (e.g., carBA- or 200 mg 2 times/day (primary tonic-
Mazepine, phenytoin, rifAMPin) may clonic). Maximum: 400 mg/day. CHIL-
decrease concentration/effect. Carbonic DREN 2–16 YRS: Initially, 1–3 mg/kg/day
anhydrase inhibitors may increase risk to maximum of 25 mg at night for 1 wk.
of kidney stone formation and severity of May increase by 1–3 mg/kg/day at wkly
metabolic acidosis. May decrease effective- intervals given in 2 divided doses. Main-
ness of oral contraceptives. Salicylates tenance: 5–9 mg/kg/day in 2 divided
(e.g., aspirin), thiazide diuretics (e.g., doses. ADULTS, ELDERLY: (Extended-Re-
hydrochlorothiazide) may increase lease): Initially, 25–50 mg/day. Increase
concentration/effect. HERBAL: Herbals by 25–50 mg/day at wkly intervals, up
with sedative properties (e.g., chamo- to 400 mg/day. CHILDREN 2 YRS AND
mile, kava kava, valerian) may increase OLDER: Initially, 25 mg (based on range
CNS depression. FOOD: None known. LAB of 1–3 mg/kg) once daily at bedtime for
VALUES: May reduce serum bicarbonate, 1 wk. Increase dose by 1–3 mg/kg at 1–2
increase ALT, AST. wk intervals up to 5–9 mg/kg once daily.

AVAILABILITY (Rx) Monotherapy with Partial-Onset, Tonic-


Clonic Seizures
Capsules (Sprinkle): 15 mg, 25 mg.
PO: ADULTS, ELDERLY, CHILDREN 10 YRS
Tablets: (Topamax): 25 mg, 50 mg, 100
AND OLDER: (Immediate-Release): Ini-
mg, 200 mg.
tially, 25 mg twice daily. May increase at
Capsules, Extended-Release: (Tro- wkly intervals up to 400 mg/day accord-
kendi XR): 25 mg, 50 mg, 100 mg, 200 ing to the following schedule: Wk 1, 25
mg. (Qudexy XR): 25 mg, 50 mg, 100 mg, mg twice daily. Wk 2, 50 mg twice daily.
150 mg, 200 mg. Wk 3, 75 mg twice daily. Wk 4, 100 mg
ADMINISTRATION/HANDLING twice daily. Wk 5, 150 mg twice daily.
Wk 6, 200 mg twice daily. CHILDREN 2–9
PO YRS: Initially, 25 mg/day. Then 25 mg 2
• Do not break, crush, dissolve, or di- times/day wk 2; then increase by 25–50
vide tablets (bitter taste). • Give with- mg/day at wkly intervals up to minimum
out regard to food. • Sprinkle capsules dose. (See table below.) ADULTS, ELDERLY,
may either be swallowed whole or con-
T tents sprinkled on teaspoonful of soft
CHILDREN 10 YRS OR OLDER: (Extended-
Release): (Qudexy XR, Trokendi
food and swallowed immediately; do not XR): Initially, 50 mg once daily. Increase
chew. • (Trokendi XR): Give whole. Do by 50 mg/day at wkly intervals for first 4
not sprinkle on food, chew, or crush. wks, then by 100 mg/day for wks 5 and 6,
(Qudexy XR): Swallow whole; may open up to 400 mg/day. CHILDREN 2–9 YRS: (Qu-
and sprinkle on spoonful of soft food. dexy XR): 6–9 YRS: (Trokendi XR): Ini-
tially, 25 mg once daily in evening. May
INDICATIONS/ROUTES/DOSAGE increase to 50 mg once daily in wk 2,
Note: Do not abruptly discontinue; ta- then 25–50 mg/day at wkly intervals over
per gradually to prevent rebound effects. 5–7 wks up to Minimum daily dose: (32
KG OR MORE): 250 mg; (12–31 KG): 200
Adjunctive Treatment of Partial-Onset
mg; (11 KG OR LESS): 150 mg. Maximum
Seizures, Lennox-Gastaut Syndrome
daily dose: (38 KG OR MORE): 400 mg;
(LGS), Tonic-Clonic Seizures
(23–38 KG): 350 mg; (12–22 KG): 300 mg;
PO: ADULTS, ELDERLY, CHILDREN 17 YRS
(11 KG OR LESS): 250 mg.
AND OLDER: (Immediate-Release):

underlined – top prescribed drug


topiramate 1165
Wgt. Minimum Maximum word-finding difficulties), memory
11 kg or 150 mg/day 250 mg/day disturbances occur occasionally. Meta-
less in 2 divided in 2 divided bolic acidosis, suicidal ideation occur
doses doses rarely.
12–22 kg 200 mg/day 300 mg/day
in 2 divided in 2 divided NURSING CONSIDERATIONS
doses doses
23–31 kg 200 mg/day 350 mg/day BASELINE ASSESSMENT
in 2 divided in 2 divided Seizures: Review history of seizure
doses doses
32–38 kg 250 mg/day 350 mg/day
disorder (intensity, frequency, duration,
in 2 divided in 2 divided level of consciousness). Initiate seizure
doses doses precautions. Provide quiet, dark environ-
39 kg or 250 mg/day 400 mg/day ment. Question for sensitivity to topira-
greater in 2 divided in 2 divided mate, pregnancy, use of other anticon-
doses doses vulsant medication (esp. carBAMazepine,
valproic acid, phenytoin). Migraine:
Migraine Prevention Assess pain location, duration, intensity.
PO: ADULTS, ELDERLY, CHILDREN 12 YRS AND Assess renal function.
OLDER: (Immediate-Release): Initially,
INTERVENTION/EVALUATION
25 mg/day. May increase by 25 mg/day at
7-day intervals up to a total daily dose of 100 Observe frequently for recurrence of sei-
mg/day in 2 divided doses. (Extended- zure activity. Assess for clinical improve-
Release): [Qudexy XR]: Initially, 25 mg ment (decrease in intensity/frequency of
once daily at bedtime. May increase wkly by seizures). Monitor renal function tests,
25 mg increments up to 100 mg once daily. LFT. Assist with ambulation if dizziness
occurs.
Dosage in Renal Impairment
PATIENT/FAMILY TEACHING
Reduce drug dosage by 50% and titrate
more slowly in pts who have CrCl less • Avoid tasks that require alertness, mo-
than 70 mL/min. tor skills until response to drug is estab-
lished (may cause dizziness, drowsiness,
Dosage in Hepatic Impairment impaired concentration). • Drowsi-
Use caution. ness usually diminishes with continued
therapy. • Avoid use of alcohol, other
SIDE EFFECTS CNS depressants. • Do not abruptly dis-
Frequent (30%–10%): Drowsiness, dizzi- continue drug (may precipitate sei-
ness, ataxia, nervousness, nystagmus, dip- zures). • Strict maintenance of drug T
lopia, paresthesia, nausea, tremor. Occa- therapy is essential for seizure con-
sional (9%–3%): Confusion, breast pain, trol. • Do not chew, crush, dissolve, or
dysmenorrhea, dyspepsia, depression, as- divide tablets (bitter taste). • Maintain
thenia, pharyngitis, weight loss, anorexia, adequate fluid intake (decreases risk of
rash, musculoskeletal pain, abdominal renal stone formation). • Report
pain, difficulty with coordination, sinus- blurred vision, eye pain. • Report sui-
itis, agitation, flu-like symptoms. Rare cidal ideation, depression, unusual be-
(3%–2%): Mood disturbances (e.g., irrita- havior. • Use caution with activities that
bility, depression), dry mouth, aggressive may increase core temperature (expo-
behavior, impaired heat regulation. sure to extreme heat, dehydra-
tion). • Instruct pt to use alternative/
ADVERSE EFFECTS/TOXIC additional means of contraception (topi-
REACTIONS ramate decreases effectiveness of oral
Psychomotor slowing, impaired con- contraceptives).
centration, language problems (esp.
Canadian trade name Non-Crushable Drug High Alert drug
1166 topotecan
death. Acts at S phase of cell cycle. Thera-
topotecan peutic Effect: Produces cytotoxic effect.
toe-poe-tee-kan PHARMACOKINETICS
(Hycamtin) Hydrolyzed to active form after IV admin-
j BLACK BOX ALERT j Must istration. Protein binding: 35%. Excreted
be administered by personnel in urine. Half-life: 2–3 hrs (increased
trained in administration/handling in renal impairment).
of chemotherapeutic agents. Potent
immunosuppressant; severe neu- LIFESPAN CONSIDERATIONS
tropenia (absolute neutrophil count
[ANC] less than 500 cells/mm3) Pregnancy/Lactation: May cause fetal
occurs in 60% of pts. Do not admin- harm. Avoid pregnancy; breastfeeding not
ister with baseline neutrophils less recommended. Children: Safety and
than 1,500 cells/mm3 and platelets efficacy not established. Elderly: Age-
less than 100,000 cells/mm3.
Do not confuse Hycamtin with related renal impairment may require
Hycomine, Mycamine, or topote- dosage adjustment.
can with irinotecan. INTERACTIONS
uCLASSIFICATION DRUG: Live virus vaccines may potenti-
PHARMACOTHERAPEUTIC: Topoi-
ate virus replication, increase vaccine side
somerase inhibitor. CLINICAL: Anti- effects, decrease pt’s antibody response to
neoplastic. vaccine. Other bone marrow depres-
sants (e.g., cladribine) may increase risk
of myelosuppression. BCRP/ABCG2 inhib-
USES itors (e.g., omeprazole, verapamil),
Treatment of metastatic ovarian cancer, P-glycoprotein/ABCB1 inhibitors (e.g.,
relapsed or refractory small cell lung amLODIPine, digoxin) may increase
cancer, recurrent or resistant cervical concentration/effect. HERBAL: Echinacea
cancer (in combination with CISplatin). may decrease effectiveness. FOOD: None
OFF-LABEL: Treatment of central nervous known. LAB VALUES: May increase serum
system lesions/lymphoma, Ewing’s sar- bilirubin, ALT, AST, alkaline phosphatase.
coma, rhabdomyosarcoma, neuroblas- May decrease RBC, leukocyte, neutrophil,
toma, acute myeloid leukemia. platelet counts, Hgb, Hct.

PRECAUTIONS AVAILABILITY (Rx)


T Contraindications: Hypersensitivity to Injection, Powder for Reconstitution: 4
topotecan. Baseline neutrophil count less mg (single-dose vial). Injection Solu-
than 1,500 cells/mm3 and platelet count tion: 1 mg/mL (4 mL).
less than 100,000 cells/mm3, severe my- Capsules: 0.25 mg, 1 mg.
elosuppression. Cautions: Mild myelo- ADMINISTRATION/HANDLING
suppression, renal impairment, breast-
feeding, pregnancy, elderly pts. Pts at risk b ALERT c Because topotecan may be
for developing interstitial lung disease carcinogenic, mutagenic, teratogenic,
(e.g., lung cancer, pulmonary fibrosis). handle drug with extreme care during
preparation/administration.
ACTION
PO
Interacts with topoisomerase I, an enzyme • May take with or without food. • Swal-
that relieves torsional strain in DNA by low whole; do not break, crush, dissolve,
inducing reversible single-strand breaks. or divide capsule. • Do not give replace-
Prevents religation of DNA strand, result- ment dose if vomiting occurs.
ing in damage to double-strand DNA, cell
underlined – top prescribed drug
topotecan 1167

IV
to nearest 0.25 mg). For severe neu-
tropenia or prolonged neutropenia,
Reconstitution • Reconstitute each platelets less than 25,000 cells/
4-mg vial (lyophilized powder) with 4 mL mm3, recovery from Grade 3 or 4
Sterile Water for Injection. • Further di- diarrhea: Reduce dose by 0.4 mg/m2/
lute with 50–100 mL 0.9% NaCl or D5W. day for subsequent cycles.
Rate of administration • Administer IV: ADULTS, ELDERLY: 1.5 mg/m2/day for 5
as IV infusion over 30 min. • Extravasa- consecutive days q21days. Neutrophils less
tion associated with only mild local reac- than 500 cells/mm3 or platelets less
tions (erythema, ecchymosis). than 25,000 cells/mm3: Reduce dose to
Storage • Store vials (lyophilized pow- 1.25 mg/m2/day for subsequent cycles.
der) at room temperature; refrigerate di-
luted solution. Diluted solution for infu- Cervical Cancer
sion stable for 24 hrs at room temperature. IV: ADULTS, ELDERLY: 0.75 mg/m2/day for
3 days (followed by CISplatin 50 mg/m2 on
IV INCOMPATIBILITIES day 1 only). Repeat q21days (baseline neu-
Dexamethasone (Decadron), 5-fluoro- trophil count greater than 1,500 cells/mm3
uracil, mitoMYcin (Mutamycin). and platelet count greater than 100,000
cells/mm3). For severe febrile neutropenia
IV COMPATIBILITIES (neutrophils less than 1,000 cells/mm3
CARBOplatin (Paraplatin), CISplatin with temperature of 38°C) or platelet count
(Platinol AQ), cyclophosphamide (Cy- less than 25,000 cells/mm3: Reduce dose
toxan), DOXOrubicin (Adriamycin), to 0.6 mg/m2/day for subsequent cycles. If
etoposide (VePesid), gemcitabine (Gem- necessary, further decrease dose to 0.45
zar), granisetron (Kytril), ondansetron mg/m2/day. Continue for a maximum of 6
(Zofran), PACLitaxel (Taxol), palonose- cycles (in non-responders) or until disease
tron (Aloxi), vinCRIStine (Oncovin). progression or unacceptable toxicity.

INDICATIONS/ROUTES/DOSAGE Dosage in Renal Impairment


IV: No dosage adjustment is necessary in
b ALERT c Do not give topotecan if
baseline neutrophil count is less than pts with mild renal impairment (CrCl 40–60
1,500 cells/mm3 and platelet count is less mL/min). For moderate renal impairment
than 100,000 cells/mm3. For retreatment, (CrCl 20–39 mL/min), give 0.75 mg/m2.
PO: CrCl 30–49 mL/min: 1.5 mg/m2/
neutrophils should be greater than 1,000
cells/mm3, platelets greater than 100,000 day. May increase by 0.4 mg/m2/day follow-
cells/mm3, and Hgb 9 g/dL or greater. ing first cycle if no GI/hematologic toxicities T
occur. CrCl less than 30 mL/min: De-
Ovarian Carcinoma crease dose to 0.6 mg/m2/day. May in-
IV: ADULTS, ELDERLY: 1.5 mg/m2/day over crease by 0.4 mg/m2/day following first
30 min for 5 consecutive days, beginning cycle if no GI/hematologic toxicities occur.
on day 1 of 21-day course. Continue until
Dosage in Hepatic Impairment
disease progression or unacceptable tox-
icity. Neutrophils less than 500 cells/ No dose adjustment.
mm3 or platelets less than 25,000 SIDE EFFECTS
cells/mm3: Reduce dose to 1.25 mg/m2/
day for subsequent cycles. Frequent (77%–21%): Nausea, vomiting, di-
arrhea, total alopecia, headache, dyspnea.
Small Cell Lung Cancer Occasional (9%–3%): Paresthesia, consti-
PO: ADULTS, ELDERLY: 2.3 mg/m2/day for pation, abdominal pain. Rare: Anorexia,
5 days; repeat q21days (dose rounded malaise, arthralgia, asthenia, myalgia.

Canadian trade name Non-Crushable Drug High Alert drug


1168 torsemide

ADVERSE EFFECTS/TOXIC
REACTIONS torsemide
Severe neutropenia (absolute neutrophil
tore-se-myde
count [ANC] less than 500 cells/mm3)
(Demadex)
occurs in 60% of pts (develops at median
Do not confuse torsemide with
of 11 days after day 1 of initial therapy).
furosemide.
Thrombocytopenia occurs in 26% of pts.
Severe anemia (RBC count less than 8 g/ uCLASSIFICATION
dL) occurs in 40% of pts (develops at
PHARMACOTHERAPEUTIC: Loop di-
median of 15 days after day 1 of initial
uretic. CLINICAL: Antihypertensive,
therapy). Severe diarrhea may occur.
diuretic.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT USES
Offer emotional support. Assess CBC with Treatment of hypertension either alone or
differential before each dose. Myelosup- in combination with other antihyperten-
pression may precipitate life-threatening sives. (Not recommended for initial treat-
hemorrhage, infection, anemia. If platelet ment of hypertension.) Edema associated
count drops, minimize trauma to pt (e.g., with HF, hepatic/renal impairment.
IM injections, pt positioning). Premedicate PRECAUTIONS
with antiemetics on day of treatment, start-
ing at least 30 min before administration. Contraindications: Hypersensitivity to
torsemide or any sulfonylurea. Anuria,
INTERVENTION/EVALUATION hepatic coma. Cautions: Pts with cirrho-
Assess for bleeding, signs of infection, sis, hypotension, hypokalemia.
anemia. Monitor hydration status, I&O,
serum electrolytes (severe diarrhea, ACTION
vomiting are common side effects). Enhances excretion of sodium, chloride,
Monitor CBC for evidence of myelosup- potassium, water at ascending limb of
pression. Monitor renal function, LFT. loop of Henle and distal renal tubules.
Assess response to medication; provide Reduces plasma, extracellular fluid vol-
interventions (e.g., small, frequent meals; ume. Therapeutic Effect: Produces
antiemetics for nausea/vomiting). Ques- diuresis, relieves edema; lowers B/P.
tion for complaints of headache. Assess
breathing pattern for evidence of dyspnea. PHARMACOKINETICS
T
Route Onset Peak Duration
PATIENT/FAMILY TEACHING PO (diuresis) 30–60 min 1–2 hrs 6–8 hrs
• Hair loss is reversible but new hair
may have different color, texture. • Di- Rapidly, well absorbed from GI tract. Pro-
arrhea may cause dehydration, electro- tein binding: 97%–99%. Metabolized in
lyte depletion. • Antiemetic and antidi- liver. Primarily excreted in urine. Not re-
arrheal medications may reduce side moved by hemodialysis. Half-life: 2–4
effects. • Notify physician if diarrhea, hrs.
vomiting, persistent fever, bruising/
bleeding, yellowing of eyes/skin oc- LIFESPAN CONSIDERATIONS
cur. • Do not have immunizations Pregnancy/Lactation: Unknown if
without physician’s approval (drug low- drug is distributed in breast milk. Chil-
ers resistance). • Avoid contact with dren: Safety and efficacy not estab-
those who have recently received live vi- lished. Elderly: No age-related precau-
rus vaccine. tions noted.

underlined – top prescribed drug


torsemide 1169

INTERACTIONS doubling dose until the desired diuretic


DRUG: NSAIDs (e.g., ibuprofen, ketor- response is acheived. Maximum single
olac, naproxen), aspirin may increase dose: 40 mg.
risk of renal impairment. May increase risk Dosage in Renal/Hepatic Impairment
of digoxin toxicity associated with torse- No dose adjustment.
mide-induced hypokalemia. May increase
risk of lithium toxicity. Bile acid seques- SIDE EFFECTS
trants (e.g., cholestyramine), sucral- Frequent (10%–4%): Headache, dizziness,
fate may decrease absorption. May increase rhinitis. Occasional (3%–1%): Asthenia,
hyponatremic effect of desmopressin. May insomnia, nervousness, diarrhea, con-
increase concentration/effect of foscarnet. stipation, nausea, dyspepsia, edema, ECG
HERBAL: Herbals with hypertensive changes, pharyngitis, cough, arthralgia,
properties (e.g., licorice, yohimbe) or myalgia. Rare (less than 1%): Syncope,
hypotensive properties (e.g., garlic, hypotension, arrhythmias.
ginger, ginkgo biloba) may alter effects.
Licorice may increase hypokalemic effect. ADVERSE EFFECTS/TOXIC
FOOD: None known. LAB VALUES: May
REACTIONS
increase serum BUN, creatinine, uric acid. Ototoxicity may occur with too-rapid IV
May decrease serum calcium, chloride, administration or with high doses; must
magnesium, potassium, sodium. be given slowly. Overdose produces
acute, profound water loss, volume/elec-
AVAILABILITY (Rx) trolyte depletion, dehydration, decreased
Tablets: 5 mg, 10 mg, 20 mg, 100 mg. blood volume, circulatory collapse.
ADMINISTRATION/HANDLING NURSING CONSIDERATIONS
PO BASELINE ASSESSMENT
• Give without regard to food. Give with
food to avoid GI upset, preferably with Obtain serum electrolyte levels, esp. po-
breakfast (prevents nocturia). tassium. Obtain baseline weight; check
for edema. Assess lungs for crackles,
INDICATIONS/ROUTES/DOSAGE signs of HF. Obtain B/P.
Hypertension INTERVENTION/EVALUATION
PO: ADULTS, ELDERLY: Initially, 2.5–5 mg/
Monitor B/P, serum electrolytes (esp. po-
day. May increase to 10 mg/day if no re-
tassium), I&O, weight. Notify physician
sponse in 4–6 wks. Range: 5–10 mg/day.
of any hearing abnormality. Note extent
T
Edema Associated with HF of diuresis. Assess lungs for rales. Check
PO: ADULTS, ELDERLY: Initially, 10–20 for signs of edema, particularly of depen-
mg/day. May increase by approximately dent areas. Although less potassium is
doubling dose until desired therapeutic lost with torsemide than with furosemide,
effect is attained. Maximum: 200 mg. assess for signs of hypokalemia (change of
muscle strength, tremor, muscle cramps,
Edema Associated with Chronic Renal altered mental status, cardiac arrhythmias).
Failure
PO: ADULTS, ELDERLY: Initially, 20 mg/ PATIENT/FAMILY TEACHING
day. May increase by approximately dou- • Take medication in morning to prevent
bling dose until desired therapeutic effect nocturia. • Expect increased urinary
is attained. Maximum: 200 mg/day. volume, frequency. • Report palpita-
tions, muscle weakness, cramps, nausea,
Edema Associated with Hepatic Cirrhosis dizziness. • Do not take other medica-
PO: ADULTS, ELDERLY: Initially, 5–10 tions (including OTC drugs) without con-
mg once daily. May increase gradually by sulting physician. • Eat foods high in
Canadian trade name Non-Crushable Drug High Alert drug
1170 trabectedin
potassium such as whole grains (cereals), continuation. Breastfeeding not recom-
legumes, meat, bananas, apricots, orange mended. Males: Male pts with female
juice, potatoes (white, sweet), raisins. partners of reproductive potential should
use barrier methods, abstinence during
trabectedin treatment and up to 5 mos after discon-
tinuation. May impair fertility in both fe-
tra-bek-te-din males and males. Children: Safety and
(Yondelis) efficacy not established. Elderly: Safety
and efficacy not established.
uCLASSIFICATION
PHARMACOTHERAPEUTIC: Alkylat- INTERACTIONS
ing agent. CLINICAL: Antineoplastic. DRUG: Strong CYP3A inducers (e.g.,
carBAMazepine, PHENobarbital, ri-
fAMPin) may decrease concentration/
USES
effect. Strong CYP3A inhibitors (e.g.,
Treatment of unresectable or metastatic clarithromycin, ketoconazole) may in-
soft tissue sarcoma (liposarcoma or leio- crease concentration/effect. Alcohol may
myosarcoma) in pts who have received a increase hepatotoxic effect. May decrease
prior anthracycline-containing regimen. therapeutic effect; increase adverse effects
of vaccines (live). HERBAL: Echinacea
PRECAUTIONS
may decrease therapeutic effect. FOOD:
Contraindications: Hypersensitivity reac- None known. LAB VALUES: May decrease
tion, anaphylactic reaction to trabectedin. Hgb, Hct, platelets, neutrophils, RBCs; se-
Cautions: Baseline anemia, neutropenia, rum albumin, phosphate. May increase se-
thrombocytopenia; chronic liver disease, rum alkaline phosphatase, ALT, AST, biliru-
cirrhosis, hepatic impairment, hepatitis; re- bin, CPK, creatinine. May reduce diagnostic
nal impairment; history of DVT, pulmonary effect of Coccidioides immitis skin test.
embolism; recent MI, cardiomyopathy, HF.
Concomitant use of strong CYP3A inducers, AVAILABILITY (Rx)
strong CYP3A inhibitors not recommended.
Powder for Reconstitution: 1 mg.
ACTION
ADMINISTRATION/HANDLING
Binds to guanine residues in the minor
groove of DNA, leading to cell cycle IV
disruption and cellular death. Blocks
­ Reconstitution • Contents are hazard-
T cell cycle at G2/M phase. Therapeutic ous; use cytotoxic precautions during han-
Effect: Inhibits tumor cell growth and dling and disposal. • Reconstitute with
metastasis. 20 mL Sterile Water for Injection for final
concentration of 0.05 mg/mL. • Shake
PHARMACOKINETICS until fully dissolved. • Visually inspect
Widely distributed. Metabolized in liver. Pro- solution for particulate matter or discolor-
tein binding: 97%. Excreted in feces (58%), ation. Solution should appear clear, color-
urine (6%). Hemodialysis not expected to less to pale brownish-yellow in color. Dis-
enhance elimination. Half-life: 175 hrs. card if solution is discolored or particles
are observed. • Dilute in 500 mL 0.9%
LIFESPAN CONSIDERATIONS NaCl or D5W bag. • See manufacturer
Pregnancy/Lactation: Avoid preg- guidelines for materials/containers that are
nancy; may cause fetal harm/malforma- compatible with diluted solution.
tions. Female pts of reproductive potential Infusion guidelines • Premedicate
should use effective contraception during with dexamethasone 20 mg IV (or appro-
treatment and up to 2 mos after dis- priate corticosteroid) 30 min prior to each
underlined – top prescribed drug
trabectedin 1171
infusion. • Infuse diluted solution imme- Serum alkaline phosphatase greater
diately after reconstitution. • Use an in- than 2.5 times ULN; serum ALT/AST
line, 0.2-micron polyethersulfone fil- greater than 5 times ULN; total se-
ter. • Infuse via dedicated central venous rum bilirubin greater than ULN: De-
line using an infusion pump. lay next dose for up to 3 wks, then re-
Rate of administration • Infuse over sume at reduced dose level.
24 hrs.
Storage • Refrigerate unused vi- Hematologic Toxicity
als. • Diluted solution must be admin- Absolute neutrophil count (ANC) less
istered within 30 hrs of reconstitution. than 1,500 cells/mm3: Delay next dose
for up to 3 wks. ANC less than 1,000
IV INCOMPATIBILITIES cells/mm3 with fever or infection;
Do not mix or infuse with other medications. ANC less than 500 cells/mm3 lasting
more than 5 days: Delay next dose for
INDICATIONS/ROUTES/DOSAGE up to 3 wks, then resume at reduced dose
Liposarcoma, Leiomyosarcoma level. Platelet count less than 100,000
IV infusion: ADULTS, ELDERLY: 1.5 mg/ cells/mm3: Delay next dose for up to 3
m2 once q3wks until disease progression wks. Platelet count less than 25,000
or unacceptable toxicity. cells/mm3: Delay next dose for up to 3
wks, then resume at reduced dose level.
Dosage in Renal Impairment
CrCl greater than or equal to 30 mL/ Nonhematologic Toxicity
min or greater: No dose adjustment. CPK greater than 2.5 times ULN: De-
CrCl greater less than 30 mL/min or lay next dose for up to 3 wks. CPK
end-stage renal disease: Not speci- greater than 5 times ULN: Delay next
fied; use caution. dose for up to 3 wks, then resume at re-
duced dose level.
Dosage in Hepatic Impairment Decreased LVEF less than lower
Mild impairment: No dose adjust- limit of normal or clinical evidence
ment. Moderate impairment: 0.9 of cardiomyopathy: Delay next dose
mg/m2 once q3wks. Severe impair- for up to 3 wks. Decreased LVEF with
ment: Not recommended. an absolute decrease of 10% or
more from baseline and less than
Dose Reduction for Normal Hepatic lower limit of normal, or clinical
Function or Mild Hepatic Impairment evidence of cardiomyopathy: Delay
Initial dose: 1.5 mg/m2 once q3wks. next dose for up to 3 wks, then resume at
First dose reduction: 1.2 mg/m2 once
T
reduced dose level.
q3wks. Second dose reduction: 1 Any other Grade 3 or 4 reaction: De-
mg/m2 once q3wks. lay next dose for up to 3 wks, then re-
sume at reduced dose level.
Dose Reduction for Moderate Hepatic
Impairment Permanent Discontinuation
Initial dose: 0.9 mg/m2 once q3wks. Permanently discontinue for persistent
First dose reduction: 0.6 mg/m2 once adverse effects requiring a delay of treat-
q3wks. Second dose reduction: 0.3 ment for more than 3 wks; continued
mg/m2 once q3wks. adverse effects after reducing dose to 1
mg/m2 in pts with normal hepatic func-
Dose Modification tion, or 0.3 mg/m2 in pts with preexist-
Hepatotoxicity ing moderate hepatic impairment; severe
Serum ALT/AST greater than hepatic dysfunction with bilirubin 2 times
2.5 times upper limit of normal ULN, and ALT/AST 3 times ULN, and alka-
(ULN): Delay next dose for up to 3 wks. line phosphatase less than 2 times ULN in
Canadian trade name Non-Crushable Drug High Alert drug
1172 trabectedin
prior treatment cycle in pts with baseline INTERVENTION/EVALUATION
normal hepatic function; exacerbation of Monitor ANC, CBC for anemia, neutro-
hepatic dysfunction in pts with preexist- penia, thrombocytopenia; CPK, serum
ing moderate hepatic impairment. creatinine for rhabdomyolysis, renal
failure; LFT for hepatotoxicity; BMP for
SIDE EFFECTS electrolyte imbalance (esp. in pts with
Frequent (75%–25%): Nausea, fatigue, as- diarrhea, vomiting, malnutrition); vital
thenia, malaise, vomiting, decreased ap- signs. Assess LVEF by echocardiogram at
petite, constipation, diarrhea, peripheral 2- to 3-mo intervals (or more frequently
edema, dyspnea, headache. Occasional in pts with cardiomyopathy). Diligently
(15%–11%): Insomnia, arthralgia, myal- screen for infections, sepsis. Monitor for
gia, paresthesia. DVT (leg or arm pain/swelling), rhab-
domyolysis (decreased urinary output,
ADVERSE EFFECTS/TOXIC amber-colored urine, fatigue, muscle
REACTIONS pain/weakness), pulmonary embolism
Anemia, neutropenia, thrombocytopenia (sudden chest pain, dyspnea, hypoxia,
are expected responses to therapy. Life- tachycardia), HF (dyspnea, fatigue, pal-
threatening, sometimes fatal, neutropenic pitations, edema, exercise intolerance);
sepsis (3% of pts) may occur. Grade 3 or hypersensitivity reaction; side effects of
4 neutropenia (43% of pts), febrile neu- dexamethasone (e.g., hyperglycemia,
tropenia (5% of pts) were reported. Fatal weight loss, decreased appetite). Moni-
rhabdomyolysis, muscular toxicity may tor I&O. Monitor daily pattern of bowel
result in renal failure. CPK elevation oc- activity, stool consistency.
curred in 32% of pts; Grade 3 or 4 CPK PATIENT/FAMILY TEACHING
elevation occurred in 6% of pts. Hepatotox-
icity, including hepatic failure, may occur. • Treatment may depress your immune
LFT elevation occurred in 70%–90% of pts. system and reduce your ability to fight in-
Cardiomyopathy including decreased ejec- fection. Report symptoms of infection
tion fraction, diastolic dysfunction, HF, right such as body aches, chills, cough, fatigue,
ventricular dysfunction reported in 6% of fever. Avoid those with active infec-
pts; Grade 3 or 4 cardiomyopathy reported tion. • Blood levels, echocardiograms
in 4% of pts. Drug extravasation may result will be routinely monitored. • Life-
in tissue necrosis requiring debridement. threatening events, such as heart failure
Other adverse effects may include phlebitis (shortness of breath, fast or slow heart
(15% of pts), pulmonary embolism (less rate, exercise intolerance, swelling of the
T ankles or legs), liver injury or failure
than 10% of pts), hypersensitivity reaction.
(abdominal pain, easy bruising, clay-col-
NURSING CONSIDERATIONS ored stools, dark-amber urine, fatigue,
loss of appetite, yellowing of skin or eyes),
BASELINE ASSESSMENT muscle toxicity (muscle pain/weakness,
Obtain ANC, CBC, CPK, BMP, LFT; vital kidney failure), blood clots in lungs (dif-
signs prior to each dose and periodically ficulty breathing, fast heart rate, chest
thereafter. Obtain baseline echocardio- pain), may occur. • Avoid pregnancy.
gram to assess LVEF. Verify placement of Female pts of childbearing potential
central venous line. Receive full medi- should use effective contraception during
cation history. Assess nutritional status. treatment and for at least 2 mos after last
Question history of DVT, pulmonary em- dose. Do not breastfeed. Male pts with fe-
bolism, cardiac disease, recent MI; renal/ male partners of reproductive potential
hepatic impairment; prior hypersensitiv- should use condoms during sexual activity
ity reaction. Screen for active infection. for at least 5 mos after last dose. • Treat-
Offer emotional support. ment may impair fertility. • Avoid grape-
underlined – top prescribed drug
traMADol 1173
fruit products, herbal supplements. • Do adenoidectomy; severe respiratory depres-
not receive live vaccines. sion; acute bronchial asthma in absence
of appropriate monitoring; GI obstruction
(paralytic ileus [known or suspected]).
traMADol Concomitant use with or within 14 days
following MAOI therapy. Cautions: CNS
tram-a-dol depression, anoxia, advanced hepatic cir-
(Apo-TraMADol , ConZip, Syn- rhosis, respiratory depression, elevated ICP,
apryn FusePaq, Ultram) history of seizures or risk for seizures, he-
j BLACK BOX ALERT j Exposes patic/renal impairment, treatment of acute
pt to risks of opioid addiction, abdominal conditions, opioid-dependent
abuse, misuse. Serious, life-
threatening respiratory depression pts, head injury, myxedema, hypothyroid-
may occur. Extended-release ism, hypoadrenalism, pregnancy. Avoid use
tablets must be swallowed whole. in pts who are suicidal or addiction prone,
Crushing, chewing, or dissolving emotionally disturbed, depressed, heavy al-
of ER tablets can result in a fatal cohol users, elderly pts, debilitated pts.
overdose. May cause neonatal
opioid withdrawal syndrome. ACTION
Concomitant use of alcohol,
benzodiazepines, CNS depressants Binds to mu-opioid receptors in CNS, in-
may cause profound sedation, hibiting ascending pain pathway. Inhibits
respiratory depression, coma, reuptake of norepinephrine, serotonin,
or death. Use with any CYP3A4
inhibitor may result in increased inhibiting descending pain pathways.
concentration/effect, which may Therapeutic Effect: Reduces pain.
cause potentially fatal respiratory
depression. PHARMACOKINETICS
Do not confuse traMADol with Route Onset Peak Duration
tapentadol, Toradol, or Tran- PO Less than 1 hr 2–3 hrs 9 hrs
date, or Ultram with Ultracet.
Rapidly, almost completely absorbed af-
FIXED-COMBINATION(S) ter PO administration. Protein binding:
Ultracet: traMADol/acetaminophen 20%. Metabolized in liver (reduced in
(a non-narcotic analgesic): 37.5 pts with advanced cirrhosis). Primarily
mg/325 mg. excreted in urine. Minimally removed
by hemodialysis. Half-life: 6–7 hrs
uCLASSIFICATION (increased in renal/hepatic failure).
PHARMACOTHERAPEUTIC: Centrally T
acting synthetic opioid. CLINICAL: LIFESPAN CONSIDERATIONS
Analgesic. Pregnancy/Lactation: Crosses pla-
centa. Distributed in breast milk. Chil-
dren: Safety and efficacy not established
USES in children 16 yrs or less. Elderly: Age-
Immediate-Release: Management related renal impairment may require
of moderate to moderately severe pain. dosage adjustment.
Extended-Release: Around-the-clock
management of moderate to moderately INTERACTIONS
severe pain for extended period.
DRUG: Alcohol, other CNS depres-
PRECAUTIONS sants (e.g., LORazepam, morphine,
Contraindications: Hypersensitivity to tra- zolpidem) may increase CNS depres-
MADol, opioids. Pediatric pts under 12 sion. CYP3A4 inhibitors (e.g., clar-
yrs of age; post-op management in pts un- ithromycin, ketoconazole) may in-
der 18 yrs following tonsillectomy and/or crease concentration/effect. May increase
Canadian trade name Non-Crushable Drug High Alert drug
1174 traMADol
CNS depressant effect; decrease therapeu- SIDE EFFECTS
tic effect of carBAMazepine. CarBAM- Frequent (25%–15%): Dizziness, vertigo,
azepine may decrease concentration/ef- nausea, constipation, headache, drowsiness.
fect. Strong CYP2D6 inhibitors (e.g., Occasional (10%–5%): Vomiting, pruritus,
FLUoxetine, PARoxetine) may de- CNS stimulation (e.g., nervousness, anxiety,
crease therapeutic effect. HERBAL: Herb- agitation, tremor, euphoria, mood swings,
als with sedative properties (e.g., hallucinations), asthenia, diaphoresis,
chamomile, kava kava, valerian) dyspepsia, dry mouth, diarrhea. Rare (less
may increase CNS depression. St. John’s than 5%): Malaise, vasodilation, anorexia,
wort may decrease concentration/effect. flatulence, rash, blurred vision, urinary re-
FOOD: None known. LAB VALUES: May tention/frequency, menopausal symptoms.
increase serum creatinine, ALT, AST. May
decrease Hgb. May cause proteinuria. ADVERSE EFFECTS/TOXIC
REACTIONS
AVAILABILITY (Rx)
Seizures reported in pts receiving traMADol
Tablets, Immediate-Release: 50 mg. Sus- within recommended dosage range. May
pension, Oral: (Synapryn FusePaq): 10 have prolonged duration of action, cumula-
mg/mL. tive effect in pts with hepatic/renal impair-
Capsules, Extended-Release: 100 mg, ment, serotonin syndrome (agitation, hallu-
150 mg, 200 mg, 300 mg. Tablets, Ex- cinations, tachycardia, hyperreflexia). May
tended-Release: 100 mg, 200 mg, 300 mg. cause suicidal ideation and behavior.
ADMINISTRATION/HANDLING NURSING CONSIDERATIONS
PO
BASELINE ASSESSMENT
• Give without regard to food but con-
sistently with or without meals. • Ex- Assess onset, type, location, duration of
tended-Release: Swallow whole; do not pain. Assess drug history, esp. carBAMaze-
break, crush, dissolve, or divide. pine, analgesics, CNS depressants, MAOIs.
Review past medical history, esp. epilepsy,
INDICATIONS/ROUTES/DOSAGE seizures. Assess renal function, LFT.
Moderate to Moderately Severe Pain
INTERVENTION/EVALUATION
PO: (Immediate-Release): ADULTS,
ELDERLY, CHILDREN 17 YRS AND OLDER: 50–
Monitor pulse, B/P, renal/hepatic func-
100 mg q4–6h. Maximum: 400 mg/day tion. Assist with ambulation if dizziness,
for pts 75 yrs and younger; 300 mg/day vertigo occurs. Dry crackers, cola may
T for pts older than 75 yrs. relieve nausea. Palpate bladder for urinary
PO: (Extended-Release): ADULTS, EL- retention. Monitor daily pattern of bowel
DERLY, CHILDREN 18 YRS AND OLDER: Ini- activity, stool consistency. Sips of water
tially, 100 mg once daily. Titrate q5days. may relieve dry mouth. Assess for clini-
Maximum: 300 mg once daily. cal improvement, record onset of relief of
pain. Monitor closely for misuse or abuse.
Dosage in Renal Impairment
PATIENT/FAMILY TEACHING
(Immediate-Release): For pts with
CrCl less than 30 mL/min, increase • May cause physical dependence. • Pts
­dosing interval to q12h. Maximum: 200 with history of drug abuse are at increased
mg/day. Do not use extended-release. risk for misuse or abuse. Take medication
only as prescribed. • Avoid alcohol, other
Dosage in Hepatic Impairment narcotics, sedatives. • May cause drowsi-
(Immediate-Release): Cirrhosis: Dos- ness, dizziness, blurred vision. • Avoid
age is decreased to 50 mg q12h. Do not tasks requiring alertness, motor skills until
use extended-release with severe hepatic response to drug is established. • Report
impairment.
underlined – top prescribed drug
trametinib 1175
severe constipation, difficulty breathing, PHARMACOKINETICS
excessive sedation, seizures, muscle weak- Rapidly absorbed after PO adminis-
ness, tremors, chest pain, palpitations. tration. Protein binding: 97.4%. Peak
plasma concentration: 1.5 hrs. Metabo-
lized in liver. Excreted in feces (80%),
urine (20%). Half-life: 3.9–4.8 days.
trametinib
LIFESPAN CONSIDERATIONS
tra-me-ti-nib Pregnancy/Lactation: Avoid pregnancy.
(Mekinist) May cause fetal harm. Must use e­ffective
Do not confuse trametinib with nonhormonal contraception dur­ing treat-
imatinib or tipifarnib. ment and for at least 4 wks after discon-
uCLASSIFICATION
tinuation (intrauterine device, barrier
methods). Unknown if distributed in breast
PHARMACOTHERAPEUTIC: MEK milk. Must either discontinue breastfeeding
­inhibitor. CLINICAL: Antineoplastic. or discontinue treatment. Children: Safety
and efficacy not established. Elderly:
May have increased risk of adverse ef-
USES fects, skin lesions, primary malignancies.
Used as a single agent or in combina- Males: May decrease spe­rm count.
tion with dabrafenib for treatment of
unresectable or metastatic melanoma INTERACTIONS
with BRAF V600E or V600L mutations, DRUG: None significant. HERBAL: None
as detected by FDA-approved test. Single- known. FOOD: High-fat meals may de-
agent regimen is not indicated in pts crease absorption/effect. LAB VALUES:
who have received prior BRAF-inhibitor Single regimen: May increase serum
therapy. Adjuvant treatment of mela- alkaline phosphatase, ALT, AST. May de-
noma in combination with dabrafenib crease serum albumin; Hgb, Hct. Com-
in pts with BRAF V600E or BRAF V600K bination regimen: May increase serum
mutations and lymph node involvement, alkaline phosphatase, ALT, AST, bilirubin,
following complete resection. Treatment calcium, creatinine, glucose, GGT, po-
of locally advanced or metastatic ana- tassium. May decrease Hgb, Hct, leuko-
plastic thyroid cancer (in combination cytes, lymphocytes, neutrophils, platelets;
with dabrafenib). Treatment of metastatic serum albumin, calcium, magnesium,
non–small-cell lung cancer (NSCLC) in phosphorus, potassium, sodium.
T
pts with BRAF V600E mutation in combi-
nation with dabrafenib. AVAILABILITY (Rx)
Tablets: 0.5 mg, 2 mg.
PRECAUTIONS
Contraindications: Hypersensitivity to ADMINISTRATION/HANDLING
trametinib. Cautions: Cardiac/pulmonary PO
impairment, preexisting diabetes or dia- • Administer at least 1 hr before or 2
betes. hrs after meal.
ACTION INDICATIONS/ROUTES/DOSAGE
Inhibits mitogen-activated extracellular Melanoma (Metastatic or Unresectable)
kinase (MEK). MEK is a downstream PO: ADULTS/ELDERLY: 2 mg once daily
effector of protein kinase Braf (BRAF). (either as a single agent or in combination
Therapeutic Effect: Inhibits cell pro- with dabrafenib). Continue until disease
liferation and causes cell cycle arrest. progression or unacceptable toxicity.

Canadian trade name Non-Crushable Drug High Alert drug


1176 trametinib
Melanoma (Adjuvant Treatment) rafenib until fever resolved, then resume
PO: ADULTS, ELDERLY: 2 mg once daily at either same dose or lower dose level.
(in combination with dabrafenib). Con- FEVER GREATER THAN 104ºF OR FEVER COM-
tinue for up to 1 yr in absence of disease PLICATED BY DEHYDRATION, HYPOTENSION,
progression or unacceptable toxicity. RENAL FAILURE: Withhold trametinib until
Thyroid Cancer resolved, then resume at either same dose
PO: ADULTS, ELDERLY: 2 mg once daily (in or lower dose level. Withhold dabrafenib
combination with dabrafenib). Continue until resolved, then resume at either lower
until disease progression or unacceptable dose level or discontinue.
toxicity. New primary malignancies: CUTANE-
OUS: No changes required for either reg-
NSCLC (Metastatic) imen. NONCUTANEOUS: Do not change
PO: ADULTS, ELDERLY: 2 mg once daily trametinib dose. Discontinue dabrafenib
in combination with dabrafenib. Continue in pts who develop RAS mutation-positive
until disease progression or unacceptable malignancies.
toxicity. Nonspecific adverse reactions: IN-
TOLERABLE GRADE 2 OR ANY GRADE 3: With-
Dose Reduction Schedule hold both regimens until resolved to Grade
Trametinib regimen: FIRST DOSE RE- 0–1, then resume at lower dose level. Dis-
DUCTION: 1.5 mg once daily. SECOND continue both regimens if not improved.
DOSE REDUCTION: 1 mg once daily. Dis- FIRST OCCURRENCE OF ANY GRADE 4 REAC-
continue if unable to tolerate 1-mg dose. TIONS: Withhold both regimens until re-
Dabrafenib combination regimen: solved to Grade 0–1, then resume at lower
FIRST DOSE REDUCTION: 100 mg twice dose level or discontinue.
daily. SECOND DOSE REDUCTION: 75 mg Ocular toxicities: GRADE 2–3 RETINAL
twice daily. THIRD DOSE REDUCTION: 50 PIGMENT EPITHELIAL DETACHMENTS: With-
mg twice daily. Discontinue if unable to hold trametinib up to 3 wks. If improved
tolerate 50-mg dose. to Grade 0–1, resume at lower dose
level. Discontinue if not improved. Do
Dose Modification not modify dabrafenib. RETINAL VEIN OC-
Based on Common Terminology Criteria CLUSION: Discontinue trametinib. Do
for Adverse Events (CTCAE) grading 1–4. not modify dabrafenib. UVEITIS OR IRI-
Cardiac: ASYMPTOMATIC DECREASE IN TIS: Do not modify trametinib. Withhold
LEFT VENTRICULAR EJECTION FRACTION dabrafenib for up to 6 wks. If improved
(LVEF) GREATER THAN 10% FROM BASE- to Grade 0–1, then resume at same dose
T LINE: Withhold trametinib up to 4 wks. level. Discontinue if not improved.
If LVEF improved, resume at lower dose Pulmonary: INTERSTITIAL LUNG DIS-
level. Discontinue if not improved. Do EASE: Discontinue trametinib. Do not
not modify dabrafenib dose. SYMPTOM- modify dabrafenib.
ATIC HF OR DECREASE IN LVEF GREATER Venous thromboembolism: UNCOM-
THAN 20% FROM BASELINE: Discontinue PLICATED DVT OR PE: Withhold trametinib
trametinib. Withhold dabrafenib until im- for up to 3 wks. If improved to Grade
proved, then resume at lower dose level. 0–1, then resume at lower dose level.
Cutaneous events: INTOLERABLE GRADE 2 Discontinue if not improved. Do not
SKIN TOXICITY OR GRADE 3–4 TOXICITY: With- modify dabrafenib. LIFE-THREATENING
hold both regimens for up to 3 wks. If im- PE: Discontinue both regimens.
proved, resume both at lower dose level.
Discontinue both regimens if not improved. Dosage in Renal/Hepatic Impairment
Febrile events: FEVER OF 101.3ºF–104ºF: Do No dose adjustment.
not modify trametinib dose. Withhold dab-

underlined – top prescribed drug


trametinib 1177

SIDE EFFECTS hypertension, rhabdomyolysis. May pro-


Single Regimen long QT interval of cardiac cycle.
Frequent (57%–32%): Rash, diarrhea, lym­
NURSING CONSIDERATIONS
phedema, peripheral edema. Occasional
(19%–10%): Dermatitis acneiform, hyper- BASELINE ASSESSMENT
tension, stomatitis, mouth ulceration, mu- Obtain baseline CBC, serum metabolic
cosal ulceration, abdominal pain, dry skin, panel (with LFT), magnesium, phosphate,
pruritus, paronychia, folliculitis, cellulitis, ionized calcium, capillary glucose level, vital
dizziness, dysgeusia, blurred vision, dry eye. signs. Obtain BRAF V600E mutation history,
negative pregnancy status, ophthalmologic
Combination Regimen exam with visual acuity, echocardiogram,
Frequent (71%–40%): Pyrexia, chills, fa- ECG before initiating treatment. Assess skin
tigue, rash, nausea, vomiting. Occasional for moles, lesions, papillomas. Question
(36%–11%): Diarrhea, abdominal pain, current breastfeeding status. Receive full
peripheral edema, headache, cough, ar- medication history including herbal prod-
thralgia, night sweats, myalgia, constipa- ucts. Question any history as listed in Pre-
tion, decreased appetite, back pain, dry cautions. Offer emotional support.
skin, insomnia, dermatitis acneiform,
dizziness, muscle spasm, extremity pain, INTERVENTION/EVALUATION
actinic keratosis, erythema, oral/throat Offer emotional support. Monitor CBC, se-
pain, urinary tract infection, pruritus, dry rum electrolytes, capillary blood glucose,
mouth, dehydration. stool characteristics routinely. Monitor for
signs of hyperglycemia (thirst, polyuria,
ADVERSE EFFECTS/TOXIC confusion, dehydration). Assess skin for
REACTIONS new lesions, toxicities every 2 mos dur-
Primary malignancies including basal or ing treatment and at least 6 mos after
squamous cell carcinoma, keratoacan- discontinuation. Obtain LVEF by echocar-
thoma, pancreatic adenocarcinoma, glio- diogram 1 mo after initiation, then every
blastoma (brain cancer) reported. DVT, 2–3 mos; ophthalmologic exam with any
PE reported in 9% of pts. May increase vision changes. Immediately report any
cell proliferation of wild-type BRAF mela- altered mental status, bleeding events, vi-
noma or new malignant melanomas. Seri- sion changes, eye pain/swelling/infection,
ous, sometimes fatal intracranial or gas- fever, urinary changes. Screen for bleed-
tric bleeding occurred in 5% of pts. Other ing of any kind. If dyspnea or leg swelling
hemorrhagic events may include con- occurs, contact physician and initiate ap-
junctival/gingival/rectal/hemorrhoidal/ propriate medical therapy (may require T
vaginal bleeding, epistaxis (nosebleed), oxygen therapy, ECG, or radiologic test to
melena (bloody stools). Cardiomyopathy, rule out DVT, PE, or ILD).
HF, decreased LVEF reported in 7%–9%
PATIENT/FAMILY TEACHING
of pts. Ocular toxicities such as retinal
vein occlusion, retinal detachment, vision • Blood work, cardiac function tests, eye
loss, glaucoma, uveitis, iritis reported. exams will be performed routinely. • Treat-
Cough, dyspnea, hypoxia, pleural effu- ment may lead to heart failure, vision
sion, infiltrates may indicate interstitial changes, lung complications, difficulty
lung disease. Serious febrile reactions breathing, fever, skin t­oxicities (such as se-
may lead to renal failure, severe dehydra- vere rash, peeling), high blood pressure,
tion, hypotension, rigors. Skin toxicities severe diarrhea. • Report bloody stools/
including palmar-plantar erythrodyses- urine, heavy menstruation, or nose-
thesia syndrome (PPES), papilloma have bleeds. • Do not breastfeed. • Avoid
occurred. Hyperglycemia reported in pregnancy; nonhormonal contraception
2%–5% of pts. Other effects may include should be used during treatment and up to 4
Canadian trade name Non-Crushable Drug High Alert drug
1178 trastuzumab
wks after treatment. • Take medication at pulmonary disease or extensive pulmo-
least 1 hr before or at least 2 hrs after meal nary tumor involvement, pregnancy.
(food reduces absorption). • Report any
increased urination, thirst, confusion (may ACTION
indicate high blood sugar); chest pain, eye Binds to extracellular domain of hu-
pain, fever, leg swelling, new skin moles or man epidermal growth factor receptor 2
lesions, vision changes. • Minimize sun- (HER2) protein, inhibiting proliferation
light exposure. • Males may experience a of tumor cells that overexpresss HER2
decreased sperm count. • Report any protein. Therapeutic Effect: Inhibits
newly prescribed medications. growth of tumor cells, mediates antibody-
dependent cellular cytotoxicity.
trastuzumab PHARMACOKINETICS
Half-life: 11–23 days.
tras-too-zoo-mab
(Herceptin) LIFESPAN CONSIDERATIONS
j BLACK BOX ALERT jAnaphy- Pregnancy/Lactation: Women should
lactic reaction, infusion reaction, use effective contraception during treatment
acute respiratory distress syndrome
have been associated with fatalities. and for at least 7 mos after discontinua-
Reduction in left ventricular ejection tion. Unknown if distributed in breast milk.
fraction, severe heart failure may Breastfeeding not recommended. Chil-
result in thrombus formation, stroke, dren: Safety and efficacy not established.
cardiac death. Exposure during Elderly: Age-related cardiac dysfunction
pregnancy may result in pulmonary
hypoplasia, skeletal malformations, may require dosage adjustment.
neonatal death.
Do not confuse trastuzumab INTERACTIONS
with ado-trastuzumab. DRUG: May increase levels/toxicity of
belimumab. May decrease concen-
uCLASSIFICATION tration/effect of paclitaxel (conven-
PHARMACOTHERAPEUTIC: HER2 tional). HERBAL: None significant.
receptor antagonist. Monoclonal an- FOOD: None known. LAB VALUES:
tibody. CLINICAL: Antineoplastic. None significant.
AVAILABILITY (Rx)
USES Injection, Powder for Reconstitution: 150
T Treatment of HER2-overexpressing mg, 440 mg.
breast cancer (adjuvant), metastatic
breast cancer, metastatic gastric or ADMINISTRATION/HANDLING
gastroesophageal junction adenocarci- IV
noma (in pts without prior treatment).
OFF-LABEL: Treatment of HER2-positive Reconstitution • Reconstitute 440-mg
metastatic breast cancer in pts who have vial with 20 mL Bacteriostatic Water for
not received prior anti-HER2 therapy or Injection (150-mg vial with 7.4 mL Sterile
in pts whose cancer has progressed on Water for Injection) to yield concentration
prior trastuzumab therapy (in combina- of 21 mg/mL. • Add calculated dose to
tion with lapatinib). 250 mL 0.9% NaCl (do not use
D5W). • Gently mix contents in bag.
PRECAUTIONS Rate of administration • Do not
Contraindications: Hypersensitivity to give IV push or bolus. • Give loading
trastuzumab. Cautions: Preexisting car- dose (4 mg/kg) over 90 min. Give
diac disease or dysfunction, preexisting

underlined – top prescribed drug


trastuzumab 1179
maintenance infusion (2 mg/kg) over monotherapy): Initially, 8 mg/kg over 90
30 min. min, then 6 mg/kg over 30–90 min q3wks
Storage • Refrigerate. • Reconsti- until disease progression.
tuted solution appears colorless to pale
yellow. • Reconstituted solution in vial Dosage Adjustment in Cardiotoxicity
is stable for 28 days if refrigerated after Left ventricular ejection fraction (LVEF)
reconstitution with Bacteriostatic Water 16% or greater decrease from baseline
for Injection (if using Sterile Water for WNL (within normal limits) or LVEF below
Injection without preservative, use im- normal limits and 10% or greater decrease
mediately; discard unused por- from baseline: Hold treatment for 4 wks.
tions). • Solution diluted in 250 mL Repeat LVEF q4wks. Resume therapy if
0.9% NaCl stable for 24 hrs if refriger- LVEF returns to normal limits in 4–8 wks
ated. and remains at 15% or less decrease from
baseline.
IV INCOMPATIBILITIES
Dosage in Renal/Hepatic Impairment
Do not mix with D5W or any other medi- No dose adjustment.
cations.
INDICATIONS/ROUTES/DOSAGE SIDE EFFECTS
Note: Do not substitute with ado- Frequent (greater than 20%): Pain, asthe-
trastuzumab emtansine. nia, fever, chills, headache, abdominal
Breast Cancer (Adjuvant)
pain, back pain, infection, nausea, diar-
IV: ADULTS, ELDERLY: (With concur- rhea, vomiting, cough, dyspnea. Occa-
sional (15%–5%): Tachycardia, HF, flu-
rent PACLitaxel or DOCEtaxel): Ini-
tially, 4 mg/kg as 90-min infusion, then like symptoms, anorexia, edema, bone
2 mg/kg wkly as 30-min infusion for 12 pain, arthralgia, insomnia, dizziness,
wks followed 1 wk later (when concur- paresthesia, depression, rhinitis, phar-
rent chemotherapy completed) by 6 mg/ yngitis, sinusitis. Rare (less than 5%): Al-
kg infusion over 30–90 min q3wks for lergic reaction, anemia, leukopenia, neu-
total therapy duration of 52 wks. (With ropathy, herpes simplex.
DOCEtaxel/CARBOplatin): Initially, 4 ADVERSE EFFECTS/TOXIC
mg/kg as 90-min infusion, then 2 mg/kg REACTIONS
wkly as 30-min infusion for a total of 18
wks, followed 1 wk later (when concur- Cardiomyopathy, ventricular dysfunction,
rent chemotherapy completed) by 6 mg/ HF occur rarely. Pancytopenia may occur.
kg infused over 30–90 min q3wks for total NURSING CONSIDERATIONS T
therapy duration of 52 wks. (Following
multimodality chemotherapy): Ini- BASELINE ASSESSMENT
tially, 8 mg/kg over 90 min, then 6 mg/kg Evaluate left ventricular function. Obtain
over 30–90 min q3wks for total of 52 wks. baseline echocardiogram, ECG, multi-
gated acquisition (MUGA) scan. Obtain
Breast Cancer (Metastatic)
CBC at baseline and at regular intervals
IV: ADULTS, ELDERLY: (Either as single during therapy.
agent or in combination with PACL­
itaxel): Initially, 4 mg/kg as 90-min in- INTERVENTION/EVALUATION
fusion, then 2 mg/kg as 30-min infusion Frequently monitor for deteriorating car-
wkly until disease progression. diac function. Assist with ambulation if as-
Gastric Cancer
thenia occurs. Monitor for fever, chills, ab-
IV: ADULTS, ELDERLY:(In combination dominal pain, back pain. Offer antiemetics
with CISplatin and either capecitabine if nausea, vomiting occur. Monitor daily
or fluorouracil for 6 cycles, then as pattern of bowel activity, stool consistency.

Canadian trade name Non-Crushable Drug High Alert drug


1180 traZODone
PATIENT/FAMILY TEACHING PHARMACOKINETICS
• Do not have immunizations without phy- Well absorbed from GI tract. Protein
sician’s approval (lowers resistance). binding: 85%–95%. Metabolized in liver.
• Avoid contact with those who have re- Primarily excreted in urine. Unknown
cently taken oral polio vaccine. • Avoid if removed by hemodialysis. Half-
crowds, those with infection. life: 5–9 hrs (increased in ­elderly).
LIFESPAN CONSIDERATIONS
traZODone Pregnancy/Lactation: Drug crosses
placenta; minimally distributed in breast
traz-o-done milk. Children: Safety and efficacy not
(Apo-TraZODone , Novo-TraZO- established in pts younger than 6 yrs.
Done ) ­ lderly: More likely to experience sed-
E
j BLACK BOX ALERT jIncreased ative, hypotensive effects; lower dosage
risk of suicidal ideation and behavior
in children, adolescents, young adults recommended.
18–24 yrs with major depressive
disorder, other psychiatric disorders. INTERACTIONS
Do not confuse traZODone with DRUG: CYP3A4 inhibitors (e.g., clar-
traMADol or ziprasidone. ithromycin, ketoconazole) may in-
crease concentration/effect. May increase
uCLASSIFICATION concentration/effect of phenytoin.
PHARMACOTHERAPEUTIC: Seroto- Strong CYP3A4 inducers (e.g., car-
nin reuptake inhibitor/antagonist. BAMazepine, rifAMPin) may decrease
CLINICAL: Antidepressant. concentration/effect. May increase QT
interval-prolonging effect of clarithro-
mycin. Linezolid, venlafaxine may in-
USES crease serotonergic effect. MAOIs (e.g.,
Treatment of major depressive disorder phenelzine, selegiline) may increase
(MDD). OFF-LABEL: Insomnia. adverse effects. HERBAL: St. John’s
wort may decrease concentration/effect.
PRECAUTIONS FOOD: None known. LAB VALUES: May
Contraindications: Hypersensitivity to decrease WBC, neutrophil counts.
traZODone. Use of MAOIs (concurrently
or within 14 days of discontinuing tra- AVAILABILITY (Rx)
ZODone or MAOI); initiation in pt re- Tablets: 50 mg, 100 mg, 150 mg,
T ceiving linezolid or IV methylene blue. 300 mg.
Cautions: Cardiac disease, arrhythmias,
cerebrovascular disease, hepatic/renal ADMINISTRATION/HANDLING
impairment, pts at high risk of suicide. PO
Conditions predisposing to priapism • Give shortly after snack, meal (re-
(e.g., sickle cell anemia); concurrent use duces risk of dizziness). • Tablets may
of antihypertensives; history of seizure be crushed.
disorder or conditions predisposing to
seizures (e.g., alcoholism); elderly pts. INDICATIONS/ROUTES/DOSAGE
b ALERT c Therapeutic effect may take
ACTION up to 6 wks to occur.
Blocks reuptake of serotonin at neuronal
presynaptic membranes, increasing its Depression
availability at postsynaptic receptor sites. PO: ADULTS: Initially, 50 mg twice daily.
Therapeutic Effect: Relieves depres- May increase in increments of 50 mg/day
sion. q3–7 days up to 75–150 mg twice daily.
underlined – top prescribed drug
trospium 1181
May further increase by 50–100 mg/day Take on empty stomach. • May take at
q2–4 wks. Usual dosage range: 200 to bedtime if drowsiness occurs. • Change
400 mg/day. Maximum: 600 mg/day. positions slowly to avoid hypotensive ef-
ELDERLY: Initially, 25–50 mg at bedtime. fect. • Avoid tasks that require alert-
May increase by 25–50 mg every 3–7 ness, motor skills until response to drug
days. Range: 75–150 mg/day. is established. • Tolerance to sedative,
anticholinergic effects usually develops
Dosage in Renal/Hepatic Impairment during early therapy. • Photosensitivity
Use caution. to sun may occur. • Dry mouth may be
relieved by sugarless gum, sips of wa-
SIDE EFFECTS ter. • Report visual disturbances, wors-
Frequent (9%–3%): Drowsiness, dry ening depression, suicidal ideation, un-
mouth, light-headedness, dizziness, head- usual changes in behavior. • Do not
ache, blurred vision, nausea, vomiting. Oc- abruptly discontinue medication.
casional (3%–1%): Nervousness, fatigue, • Avoid alcohol.
constipation, myalgia/arthralgia, mild hy-
potension. Rare: Photosensitivity reaction.
trospium
ADVERSE EFFECTS/TOXIC
REACTIONS tro-spee-um
Priapism, altered libido, retrograde ejacu- (Trosec , Sanctura XR )
lation, impotence occur rarely. Appears to
be less cardiotoxic than other antidepres- uCLASSIFICATION
sants, although arrhythmias may occur in PHARMACOTHERAPEUTIC: Anticho-
pts with preexisting cardiac disease. linergic. CLINICAL: Antispasmodic.
NURSING CONSIDERATIONS
USES
BASELINE ASSESSMENT
Treatment of overactive bladder with
Assess mental status, mood, behavior. For symptoms of urge urinary incontinence,
pts on long-term therapy, serum hepatic/ urgency, urinary frequency.
renal function tests, blood counts should
be performed periodically. Elderly pts are PRECAUTIONS
more likely to experience sedative, hypo- Contraindications: Hypersensitivity to
tensive effects. Question history as listed trospium. Pts with or at increased risk
in Precautions. of gastric retention, uncontrolled nar- T
INTERVENTION/EVALUATION row-angle glaucoma, urinary retention.
Cautions: Decreased GI motility, renal/
Monitor for suicidal ideation (esp.
at beginning of therapy or dosage hepatic impairment, obstructive GI dis-
change). Assess appearance, behavior, orders, ulcerative colitis, intestinal atony,
speech pattern, level of interest, mood. myasthenia gravis, controlled narrow-
Monitor WBC, neutrophil count, angle glaucoma, bladder flow obstruc-
hepatic enzymes. Assist with amb­ tion, Alzheimer’s disease, hot weather/
ulation if dizziness, light-headedness exercise, elderly pts.
occurs. ACTION
PATIENT/FAMILY TEACHING Antagonizes effect of acetylcholine on
• Immediately discontinue medication, muscarinic receptors, producing para-
consult physician if priapism occurs. • sympatholytic action. Therapeutic Ef-
Immediate-Release: May take after fect: Reduces smooth muscle tone in
meal, snack. • Extended-Release: bladder.

Canadian trade name Non-Crushable Drug High Alert drug


1182 trospium

PHARMACOKINETICS Dosage in Renal Impairment


CrCl less than 30 mL/min: Immediate-
Minimally absorbed after PO administra-
tion. Protein binding: 50%–85%. Distrib- release dose is reduced to 20 mg once
uted in plasma. Excreted in feces (82%), daily at bedtime. Extended-release not
urine (6%). Half-life: 20 hrs. recommended.
Dosage in Hepatic Impairment
LIFESPAN CONSIDERATIONS
Mild impairment: No dose adjustment.
Pregnancy/Lactation: Unknown if Moderate to severe impairment: Use
drug crosses placenta or is distributed with caution.
in breast milk. Children: Safety and ef-
ficacy not established. Elderly: Higher SIDE EFFECTS
incidence of dry mouth, constipation, Frequent (20%): Dry mouth. Occasional
dyspepsia, UTI, urinary retention in pts (10%–4%): Constipation, headache. Rare
75 yrs and older. (less than 2%): Fatigue, upper abdominal
INTERACTIONS pain, dyspepsia (heartburn, indigestion,
epigastric pain), flatulence, dry eyes, uri-
DRUG: Alcohol may increase CNS nary retention.
depression. Anticholinergics (e.g.,
aclidinium, ipratropium, tiotro- ADVERSE EFFECTS/TOXIC
pium, umeclidinium) may increase REACTIONS
anticholinergic effect. HERBAL: None Overdose may result in severe anticho-
significant. FOOD: High-fat meals may linergic effects, characterized by ner-
reduce absorption. LAB VALUES: None vousness, restlessness, nausea, vomiting,
significant. confusion, diaphoresis, facial flushing,
AVAILABILITY (Rx) hypertension, hypotension, respiratory
depression, irritability, lacrimation. Su-
Tablets: 20 mg. Capsules, Extended- praventricular tachycardia and hallucina-
Release: 60 mg. tions occur rarely.
ADMINISTRATION/HANDLING NURSING CONSIDERATIONS
PO
BASELINE ASSESSMENT
• Store at room temperature. • Give at
least 1 hr before meals or on an empty Assess for presence of dysuria, urinary
stomach. • Do not break, crush, dis- urgency, frequency, incontinence.
T solve, or divide tablets or extended-re- INTERVENTION/EVALUATION
lease capsules; swallow whole. • Ad-
Monitor for symptomatic relief. Monitor
minister tablets at bedtime, capsules in
I&O; palpate bladder for retention. Moni-
morning with full glass of water, 1 hr
tor daily pattern of bowel activity, stool
before eating.
consistency. Dry mouth may be relieved
INDICATIONS/ROUTES/DOSAGE by sips of tepid water.
Overactive Bladder PATIENT/FAMILY TEACHING
PO: ADULTS: (Immediate-Release): • Report nausea, vomiting, diaphoresis,
20 mg twice daily. ELDERLY 75 YRS AND increased salivary secretions, palpita-
OLDER: 20 mg once daily at bedtime. tions, severe abdominal pain. • Swal-
ADULTS, ELDERLY: (Extended-Release): low tablets, extended-release capsules
60 mg once daily in the morning. whole. • Give 1 hr before meals.

underlined – top prescribed drug


umeclidinium 1183
Peak concentration: 5–15 min. Steady
umeclidinium state reached within 14 days. Half-
life: 11 hrs.
ue-mek-li-din-ee-um
(Incruse Ellipta) LIFESPAN CONSIDERATIONS
Do not confuse umeclidinium Pregnancy/Lactation: Unknown if dis­
with aclidinium or clidinium. tributed in breast milk. Must either discon-
tinue drug or discontinue breastfeeding.
FIXED-COMBINATION(S) Children: Not indicated in this pt popula-
Anoro Ellipta: umeclidinium / tion. Elderly: No age-related precautions
vilanterol (bronchodilator): 62.5 noted.
mcg/25 mcg. Trelegy Ellipta: ume-
clidium/fluticasone (corticosteroid)/ INTERACTIONS
vilanterol (bronchodilator): 62.5 DRUG: Anticholinergics (e.g., acli­
mcg/100 mcg/25 mcg. dinium, ipratropium, tiotropium)
may increase anticholinergic effect.
uCLASSIFICATION HERBAL: None significant. FOOD: None
PHARMACOTHERAPEUTIC: Anticho- known. LAB VALUES: None known.
linergic. CLINICAL: Bronchodilator
(long-acting). AVAILABILITY (Rx)
Inhalation Powder: 62.5 mcg /capsule (in
blister packs containing 7 or 30 doses).
USES
Long-term, once-daily maintenance treat- ADMINISTRATION/HANDLING
ment of airflow obstruction in pts with Inhalation
COPD including chronic bronchitis and / Administration • Follow instructions
or emphysema. for preparation according to manufac-
turer guidelines. • Do not shake or
PRECAUTIONS prime. Prior to inhaling dose, exhale
Contraindications: Hypersensitivity to ume­ fully (do not exhale into inhaler). Close
clidinium. Severe hypersensitivity to milk lips tightly around inhaler and inhale
proteins or any drug components. Cau- (rapidly, steadily, and deeply). Do not
tions: Bladder neck obstruction, myas- breathe through nose or block air vent
thenia gravis, narrow-angle glaucoma, with fingers. • Remove mouthpiece and
prostatic hypertrophy, urinary retention. hold breath for 3–4 sec, then breathe
Not recommended in pts with acutely out slowly and gently. Do not close
deteriorating COPD requiring emergent container until medication has been in-
relief of acute symptoms. haled. • Close lid cover. U
Storage • Store at room temperature up
ACTION to 6 wks after opening tray. • Do not
Inhibits muscarinic M3 receptor in lungs, refrigerate or freeze. • Protect from
­
resulting in relaxation of bronchial smooth sunlight and moisture. • Discard after
­
muscle. Therapeutic Effect: Relieves counter reaches 0. • Do not reuse inhaler.
bronchospasm, reduces airway resis-
tance, improves bronchodilation. INDICATIONS/ROUTES/DOSAGE
COPD
PHARMACOKINETICS Inhalation: ADULTS, ELDERLY: One in-
Rapidly absorbed following inhalation. halation (62.5 mcg) once daily, at same
Primarily metabolized by enzyme cyto- time each day. Maximum: 1 inhala-
chrome P4502D6. Protein binding: 89%. tion /24 hrs.

Canadian trade name Non-Crushable Drug High Alert drug


1184 ustekinumab
Dose Modification INTERVENTION/EVALUATION
Deterioration of COPD: Discontinue Routinely monitor O2 saturation, vi-
treatment. Institute short-acting bron- tal signs. Auscultate lung sounds and
chodilators and supportive pulmonary monitor for symptom improvement.
therapy. Recommend discontinuation of short-
acting beta2-agonists while on long-
Dosage in Renal Impairment
term therapy. Monitor for COPD de-
No dose adjustment. terioration, narrow-angle glaucoma,
Dosage in Hepatic Impairment urinary retention/obstruction. Monitor
Mild to moderate impairment: No for increased use of rescue inhaler;
dose adjustment. Severe impairment: may indicate worsening of respiratory
Use caution. status.
PATIENT/FAMILY TEACHING
SIDE EFFECTS
• Report fever, productive cough, body
Occasional (8%–5%): Nasopharyngitis, aches, paradoxical bronchospasm, diffi-
upper respiratory tract infection. Rare culty breathing; may indicate lung infec-
(3%–1%): Cough, arthralgia, viral respira-
tion, worsening of COPD. • Therapy
tory tract infection, pharyngitis, myalgia, not intended for acute COPD symptom
abdominal pain, toothache, tachycardia. relief, and extra doses are not ad-
ADVERSE EFFECTS/TOXIC vised. • Report symptoms of acute
REACTIONS narrow-angle glaucoma, urinary reten-
tion, bladder distention. • Refill pre-
Life-threatening asthma-related events, scription when counter on left of inhaler
bronchospasm, worsening of COPD- reaches red area of scale. • Follow
related symptoms have been reported. manufacturer guidelines for proper use
Hypersensitivity reactions may occur of inhaler. • Drink plenty of fluids (de-
(esp. in pts with undiagnosed severe creases lung secretion viscosity).
milk protein allergy or allergy to prod- • Rinse mouth with water after inhala-
ucts containing lactose). Worsening of tion to decrease mouth/throat irritation.
narrow-angle glaucoma (eye pain, blurry
vision, visual halos, colored images in
association with red eyes from conjunc-
tival congestion and corneal edema) may
occur. May cause worsening of urinary
ustekinumab
retention, esp. in pts with prostatic hy- yoo-ste-kin-ue-mab
pertrophy or bladder neck obstruction. (Stelara)
U NURSING CONSIDERATIONS Do not confuse Stelara with
Aldara, or ustekinumab with
BASELINE ASSESSMENT inFLIXimab or riTUXimab.
Obtain baseline O2 saturation, vital signs;
pulmonary function test, if applicable. uCLASSIFICATION
Assess respiratory rate, depth, rhythm. PHARMACOTHERAPEUTIC: Inter-
Assess lung sounds for wheezing, rales. leukin-12, interleukin-23 inhibitor,
Screen for concomitant use of anticho- monoclonal antibody. CLINICAL: An-
linergic medications. Question history of tipsoriasis agent.
asthma, BPH, bladder neck obstruction,
glaucoma. Teach proper inhaler priming
and administration techniques. Conduct USES
ophthalmologic exam in pts with narrow- Treatment of adults, adolescents 12 yrs
angle glaucoma. or older with moderate to severe plaque

underlined – top prescribed drug


ustekinumab 1185
psoriasis who are candidates for systemic AVAILABILITY (Rx)
therapy or phototherapy. Treatment of Injection Solution, Intravenous: 130 mg /
adults with active psoriatic arthritis alone 26 mL. Injection Solution, SQ (Prefilled
or in combination with methotrexate. Syringes): 45 mg/0.5 mL, 90 mg/mL.
Treatment of adults with moderate to se-
vere active Crohn’s disease. ADMINISTRATION/HANDLING
IV
PRECAUTIONS
Contraindications: Hypersensitivity to us­ Reconstitution • Calculate the num-
tekinumab. Cautions: History of chronic ber of vials needed for dose based on pt’s
infection, recurrent infection, active weight. • Withdraw and discard a vol-
tuberculosis, prior malignancy, renal/ ume from 250-mL 0.9% NaCl infusion
hepatic impairment. Avoid use of live vac- bag equal to the volume of vials needed
cines. for dose. • Withdraw calculated dose
from vial or vials and add to infusion bag
ACTION to equal a final volume of 250 mL. • Vi-
Strongly binds with cellular components sually inspect for particulate matter or
involved in responses to inflammation discoloration. Do not use if solution is
and immune system, thereby decreasing cloudy, discolored, or if visible particles
likelihood of aggravating psoriatic erup- are observed.
tions. Therapeutic Effect: Significantly Rate of administration • Infuse over
slows growth, migration of circulating at least 60 min. Use an in-line, low-pro-
total lymphocytes (predominant in pso- tein-binding filter (0.2 microns).
riatic lesions). Storage • Refrigerate unused vials in
original carton until time of use. • Pro-
PHARMACOKINETICS tect from light. • Keep vials upright.
• Diluted solution may be stored at room
Following SQ injections, clearance is
temperature for up to 4 hrs.
affected by body weight, is not affected
by gender or race. Degraded into small SQ
peptides and amino acids via catabolic Preparation • Visually inspect for
pathways. Steady state reached in 28 particulate matter or discoloration. Solu-
wks. Half-life: 10–126 days. tion should appear clear and colorless to
slightly yellow in color. • Solution may
LIFESPAN CONSIDERATIONS contain a few small translucent or white
Pregnancy/Lactation: Unknown if particles.
dis­tributed in breast milk. Children: Not Administration • Insert needle sub-
indicated for use in this pt population. El- cutaneously into upper arm, outer thigh,
derly: Age-related increased incidence or abdomen and inject solution. • Do U
of infection requires cautious use. not inject into areas of active skin dis-
ease or injury such as sunburns, skin
INTERACTIONS rashes, inflammation, skin infections, or
DRUG: May increase immunosup- active psoriasis. • Do not administer
pressive effect of inFLIXimab. May IV or intramuscular. • Rotate injection
decrease therapeutic effect; increase sites.
adverse effects of vaccines (live). Storage • Refrigerate prefilled sy-
HERBAL: Echinacea may decrease con- ringes in original carton until time of
centration/effect. FOOD: None known. use. • Protect from light. • Do not
LAB VALUES: May increase lymphocyte freeze or expose to heating sources. • Do
count. not shake.

Canadian trade name Non-Crushable Drug High Alert drug


1186 ustekinumab

INDICATIONS/ROUTES/DOSAGE pain, dizziness, pruritus, injection site ery-


Plaque Psoriasis thema, myalgia, depression.
SQ: ADULTS, ELDERLY WEIGHING 100 KG
ADVERSE EFFECTS / TOXIC
OR LESS: Initially, 45 mg, then 45 mg 4
REACTIONS
wks later, followed by 45 mg every 12
wks. WEIGHING MORE THAN 100 KG: Ini- Worsening of psoriasis, thrombocyto-
tially, 90 mg, then 90 mg 4 wks later, fol- penia, malignancies, serious infections
lowed by 90 mg every 12 wks. Note: 45 (cellulitis, diverticulitis, gastroenteritis,
mg also efficacious; however, 90 mg pneumonia, osteomyelitis, UTI, postoper-
is recommended due to greater effi- ative wound infection) have been noted.
cacy. CHILDREN 12 YRS AND OLDER WEIGH- Reversible posterior leukoencepha-
ING MORE THAN 100 KG: Initially, 90 mg, lopathy syndrome (headache, seizures,
repeat in 4 wks, then q12 wks. WEIGH- confusion, visual disturbances) occurs
ING 61–100 KG: Initially, 45 mg, repeat in rarely.
4 wks, then q12 wks. WEIGHING 60 KG OR
NURSING CONSIDERATIONS
LESS: Initially, 0.75 mg/kg, repeat in 4
wks, then q12 wks. BASELINE ASSESSMENT
Pts should not receive live vaccines dur-
Psoriatic Arthritis
ing treatment, 1 yr prior to initiating
SQ: ADULTS, ELDERLY: Initially, 45 mg
treatment, or 1 yr following discontinu-
repeated in 4 wks followed by 45 mg
ation of treatment. Inform pt of duration
q12wks. PTS WITH COEXISTENT MODER-
of treatment and required monitoring
ATE TO SEVERE PLAQUE PSORIASIS WEIGH-
procedures. Assess skin prior to therapy;
ING MORE THAN 100 KG: Initially, 90 mg
document extent and location of psoria-
repeated in 4 wks, then 90 mg q12wks.
sis lesions. Test pt for tuberculosis infec-
Crohn’s Disease tion prior to initiating treatment.
IV infusion: ADULTS, ELDERLY: Initially, INTERVENTION/EVALUATION
(as a single dose) 520 mg (greater than
Closely monitor for signs / symptoms of
85 kg); 390 mg (56–85 kg); 260 mg (up
active tuberculosis during and after treat-
to 54 kg).
ment. Assess skin throughout therapy for
SQ: Maintenance: 90 mg q8wks be-
evidence of improvement of psoriasis le-
ginning 8 wks following the IV induction
sions. Monitor for worsening of lesions.
dose.
PATIENT/FAMILY TEACHING
Dosage in Renal/Hepatic Impairment
• If appropriate, pt may self-inject after
No dose adjustment.
proper training in preparation and injec-
U SIDE EFFECTS tion technique. • Report any signs of
infection. • If new diagnosis of malig-
Occasional (8%–4%): Nasopharyngitis, up-
nancy occurs, inform physician of cur-
per respiratory tract infection, headache.
rent treatment with ustekinumab.
Rare (3%–1%): Fatigue, diarrhea, back

underlined – top prescribed drug


valACYclovir 1187
LIFESPAN CONSIDERATIONS
valACYclovir Pregnancy/Lactation: May cross pla-
centa. May be distributed in breast milk.
val-a-sye-kloe-veer Children: Safety and efficacy not es-
(Valtrex) tablished in children younger than 2 yrs
Do not confuse valACYclovir (chickenpox); younger than 12 yrs (cold
with acyclovir or valGANciclovir, sores). Elderly: Age-related renal im-
or Valtrex with Valcyte. pairment may require dosage adjustment.
uCLASSIFICATION
INTERACTIONS
PHARMACOTHERAPEUTIC: Nucleo- DRUG: Nephrotoxic medications (e.g.,
side analogue DNA polymerase in- foscarnet, gentamicin) may increase risk
hibitor. CLINICAL: Antiviral. of nephrotoxicity, renal impairment. May in-
crease concentration/effect of tiZANidine.
USES HERBAL: None significant. FOOD: None
known. LAB VALUES: None significant.
Treatment of herpes zoster (shingles) in
immunocompetent pts. Treatment of ini- AVAILABILITY (Rx)
tial and recurrent genital herpes in im-
Tablets: 500 mg, 1,000 mg.
munocompetent adults. Prevention of
recurrent genital herpes and reduction of ADMINISTRATION/HANDLING
transmission of genital herpes in immu- PO
nocompetent pts. Suppression of genital • Give without regard to food. • If GI
herpes in HIV-infected pts. Treatment of upset occurs, give with meals.
herpes labialis (cold sores). Treatment
of chickenpox in immunocompetent INDICATIONS/ROUTES/DOSAGE
children. OFF-LABEL: Prophylaxis and Herpes Zoster (Shingles)
treatment of cancer-related HSV, VZV. PO: ADULTS, ELDERLY: (Immunocom-
PRECAUTIONS petent): 1 g 3 times/day for 7 days. (Im-
munocompromised): 1 g 3 times/day
Contraindications: Hypersensitivity to acy­ for 7–14 days.
clovir, valACYclovir. Cautions: Renal im-
pairment, concurrent use of nephrotoxic Herpes Simplex (Cold Sores)
agents, elderly pts. PO: ADULTS, ELDERLY: (Immunocom-
petent): 2 g twice daily for 1 day (sepa-
ACTION rate by 12 hrs). (Immunocompro-
Converted to acyclovir by intestinal/he- mised): 1 g 2 times/day for 5–10 days.
patic metabolism. Competes for viral DNA
Initial Episode of Genital Herpes
polymerase; inhibits incorporation into
PO: ADULTS, ELDERLY: (Immunocom-
viral DNA. Therapeutic Effect: Inhibits V
petent): 1 g twice daily for 10 days.
DNA synthesis and viral replication.
(Immunocompromised): 1 g 2 times/
PHARMACOKINETICS day for 5–10 days.
Rapidly absorbed after PO administra- Recurrent Episodes of Genital Herpes
tion. Protein binding: 13%–18%. Rap- PO: ADULTS, ELDERLY: (Immunocom-
idly converted by hydrolysis to active petent): 500 mg twice daily for 3 days.
compound acyclovir. Widely distributed (Immunocompromised): 1 g 2 times/
to tissues, body fluids (including CSF). day for 5–10 days.
Primarily excreted in urine. Removed by
Suppressive Therapy of Genital Herpes
hemodialysis. Half-life: Acyclovir: 2.5–
PO: ADULTS, ELDERLY: (Immunocom-
3.3 hrs (increased in renal impairment).
petent): 500 mg twice daily or 1 g once
Canadian trade name Non-Crushable Drug High Alert drug
1188 valbenazine
daily (500 mg once daily in pts with 9 or NURSING CONSIDERATIONS
fewer recurrences/yr). (Immunocom-
promised): 500 mg 2 times/day. BASELINE ASSESSMENT
Question for history of allergies, par-
Chickenpox ticularly to valACYclovir, acyclovir. Tissue
PO: CHILDREN 2–17 YRS: (Immunocom- cultures for herpes zoster, herpes simplex
petent): 20 mg/kg/dose 3 times/day for should be obtained before giving first dose
5 days. Maximum: 1 g 3 times/day. (therapy may proceed before results are
Dosage in Renal Impairment
known). Assess medical history, esp. HIV
Dosage and frequency are modified infection, bone marrow or renal trans-
based on creatinine clearance. HD: Give plantation, renal/hepatic impairment. As-
dose postdialysis. sess characteristics, frequency of lesions.
INTERVENTION/EVALUATION
Cold Sores/Herpes Zoster
Monitor CBC, LFT, renal function, urinalysis.
Creatinine Herpes
Evaluate cutaneous lesions. Provide analge-
Clearance Zoster Cold Sores
sics, comfort measures for herpes zoster
30–49 mL/min 1 g q12h 1 g q12h × (esp. exhausting to elderly). Encourage flu-
2 doses
10–29 mL/min 1 g q24h 500 mg q12h ×
ids. Keep pt’s fingernails short, hands clean.
2 doses PATIENT/FAMILY TEACHING
Less than 500 mg 500 mg as
10 mL/min q24h single dose • Drink adequate fluids. • Do not touch
lesions with fingers to avoid spreading infec-
Genital Herpes
tion to new site. • Genital herpes: Con-
Creatinine Initial Recurrent Suppressive
tinue therapy for full length of treat-
Clearance Episode Episode Therapy
ment. • Space doses evenly. • Avoid sexual
intercourse during duration of lesions to pre-
10–29 1 g q24h 500 mg 500 mg
vent infecting partner. • ValACYclovir does
mL/min q24h q24–48h
Less than 500 mg 500 mg 500 mg not cure herpes. • Report if lesions recur or
10 mL/min q24h q24h q24–48h do not improve. • Pap smears should be
done at least annually due to increased risk of
Dosage in Hepatic Impairment cervical cancer in women with genital her-
No dose adjustment. pes. • Initiate treatment at first sign of recur-
rent episode of genital herpes or herpes zoster
SIDE EFFECTS (early treatment within first 24–48 hrs is im-
Frequent: Herpes zoster (17%–10%): perative for therapeutic results).
Nausea, headache. Genital herpes
(17%): Headache. Occasional: Herpes
zoster (7%–3%): Vomiting, diarrhea,
V constipation (50 yrs and older), asthe- valbenazine
nia, dizziness (50 yrs and older). Genital
herpes (8%–3%): Nausea, diarrhea, diz- val-ben-a-zeen
ziness. Rare: Herpes zoster (3%–1%): (Ingrezza)
Abdominal pain, anorexia. Genital her- Do not confuse with carBAMaz-
pes (3%–1%): Asthenia, abdominal pain. epine, deutetrabenazine, or
tetrabenazine.
ADVERSE EFFECTS/TOXIC
uCLASSIFICATION
REACTIONS
Neutropenia, thrombocytopenia, renal PHARMACOTHERAPEUTIC: Central
failure occur rarely. monoamine-depleting agent. Vesicular
monoamine transporter-2 (VMAT2)

underlined – top prescribed drug


valbenazine 1189
inhibitor. CLINICAL: Reduces tardive avir), strong CYP2D6 inhibitors
dyskinesia. (e.g., FLUoxetine, PARoxetine) may
increase concentration/effect. Strong
CYP3A4 inducers (e.g., carBAM-
USES azepine, phenytoin, rifAMPin) may
Treatment of adults with tardive dyskinesia. decrease concentration/effect. May in-
PRECAUTIONS crease concentration/adverse effects of
MAOIs (e.g., phenelzine, selegiline).
Contraindications: Hypersensitivity to val- HERBAL: St. John’s wort may decrease
benazine. Cautions: Pts at risk for falls, concentration/effect. FOOD: None known.
severe osteoporosis; concomitant use with LAB VALUES: May increase alkaline phos-
strong CYP2D6 inhibitors, strong CYP3A4 phatase, bilirubin, prolactin, glucose.
inhibitors or in a poor CYP2D6 metabo-
lizer, QTc interval–prolonging medications. AVAILABILITY (Rx)
Pts with congenital QT syndrome, arrhyth-
mias associated with prolonged QT interval. Capsules: 40 mg, 80 mg.
Pts with depression or suicidal ideation, ADMINISTRATION/HANDLING
moderate to severe hepatic impairment.
PO
Avoid use in severe renal impairment.
• Give with or without food.
ACTION
INDICATIONS/ROUTES/DOSAGE
Exact mechanism of action for dyskinesia
unknown. Thought to be mediated by re- Tardive Dyskinesia
versible inhibition of VMAT2, a transporter PO: ADULTS, ELDERLY: 40 mg once daily.
that regulates uptake of monoamine from May increase to 80 mg once daily if toler-
the cytoplasm to the synaptic vesicle for ated after 7 days.
storage and release. Therapeutic Ef- Dose Modification
fect: Reduces abnormal involuntary CYP2D2 poor metabolizers: Consider
movements; improves motor function. reducing dose based on tolerability.
PHARMACOKINETICS Dosage in Renal Impairment
Widely distributed. High-fat meals de- Mild to moderate impairment: No
crease absorption. Metabolized by hy- dose adjustment. Severe impairment:
drolysis to active metabolite. Protein Not recommended.
binding: greater than 99%. Peak plasma
concentration: 30–60 min (metabolite: Dosage in Hepatic Impairment
4–8 hrs). Excreted in urine (60%), feces Mild impairment: No dose adjustment.
(30%). Half-life: 15–22 hrs. Moderate to severe impairment: 40
mg once daily.
LIFESPAN CONSIDERATIONS
Pregnancy/Lactation: Unknown if dis- SIDE EFFECTS V
tributed in breast milk. Breastfeeding not Occasional (13%–3%): Somnolence, fa-
recommended during treatment and for tigue, sedation, dry mouth, constipation,
at least 5 days after discontinuation. Chil- attention disturbance, blurry vision, urinary
dren: Safety and efficacy not established. retention, gait disturbance, dizziness, bal-
Elderly: No age-related precautions noted. ance disorder, vomiting. Rare (2%): mus-
culoskeletal disorders, arthralgia.
INTERACTIONS
DRUG: Deutetrabenazine, tetrabena- ADVERSE EFFECTS/TOXIC
zine may enhance adverse/toxic effects. REACTIONS
Strong CYP3A4 inhibitors (e.g., May increase risk of falls, injury. Elevated
clarithromycin, ketoconazole, riton­ serum alkaline phosphatase, bilirubin
Canadian trade name Non-Crushable Drug High Alert drug
1190 valGANciclovir
may indicate risk of cholestasis. May (Apo-ValGANciclovir , Valcyte)
cause QTc prolongation in pts who are j BLACK BOX ALERT jMay
CYP2D6 poor metabolizers or taking adversely affect spermatogenesis,
concomitant CYP2D6 inhibitors, which fertility. Risk for granulocytopenia,
may increase the risk of torsades de anemia, thrombocytopenia.
pointes, sudden cardiac death. VMAT2 Do not confuse Valcyte with
inhibitors are associated with elevated Valium or Valtrex, or valGANci-
serum prolactin levels, which may cause clovir with valACYclovir.
low estrogen levels, thereby increasing
uCLASSIFICATION
risk of amenorrhea, galactorrhea, gyne-
comastia, osteoporosis. PHARMACOTHERAPEUTIC: Synthetic
nucleoside. CLINICAL: Antiviral.
NURSING CONSIDERATIONS
BASELINE ASSESSMENT USES
Obtain baseline LFTs, ECG (pts at risk for Adults: Treatment of cytomegalovirus (CMV)
QT prolongation). Assess for depression retinitis in AIDS. Prevention of CMV disease
or suicidal ideation. Assess baseline of in high-risk renal, cardiac, renal-pancreas
abnormal involuntary movements. Re- transplant pts. Children: Prevention of CMV
ceive full medication history and screen disease in high-risk renal (4 mos to 16 yrs)
for interactions. Initiate fall precautions. and cardiac transplant pts (1 mo to 16 yrs).
Offer emotional support.
PRECAUTIONS
INTERVENTION/EVALUATION
Contraindications: Hypersensitivity to val-
Assess for clinical improvement, rever- GANciclovir, ganciclovir. Cautions: Use
sal of symptoms (lip smacking, puck- extreme caution in children due to long-
ering, tongue protrusion or chewing, term carcinogenicity, reproductive toxicity.
jaw movement, rapid blinking of the Renal impairment, concurrent nephrotoxic
eye; slow, deliberate movements; rapid medications, preexisting bone marrow sup-
jerking motion that interrupts normal pression or cytopenias, history of cytopenic
coordinated movement). Assist with reactions to other drugs, elderly pts (at
ambulation. greater risk for renal impairment).
PATIENT/FAMILY TEACHING
ACTION
• Therapy is not a cure, but it may help with
abnormal involuntary movements associated Inhibits binding of deoxyguanosine triphos-
with disease. • Do not take newly pre- phate to DNA polymerase. Therapeutic
scribed medications unless approved by Effect: Inhibits viral DNA synthesis.
prescriber that originally started treat- PHARMACOKINETICS
ment. • Report fainting, chest pain, palpita-
V tions, irregular heart rhythm. • Avoid tasks Well absorbed, rapidly converted to gan-
that require alertness, motor skills until re- ciclovir by intestinal mucosal cells and
sponse to drug is established. • Do not hepatocytes. Widely distributed includ-
breastfeed during treatment and for at least 5 ing CSF, ocular tissue. Slowly metabo-
days after final dose. lized intracellularly. Primarily excreted
in urine. Removed by hemodialysis.
Half-life: Ganciclovir: 4 hrs (in-
creased in renal impairment).
valGANciclovir LIFESPAN CONSIDERATIONS
val-gan-sye-kloe-veer Pregnancy/Lactation: Avoid pregna­
ncy; may cause fetal harm/malforma-

underlined – top prescribed drug


valGANciclovir 1191
tions. Female pts of reproductive potential Prevention of CMV After Transplant
should use effective contraception during PO: ADULTS, ELDERLY: 900 mg once
treatment. Avoid breastfeeding; may be daily beginning within 10 days of trans-
resumed no sooner than 72 hrs after last plant and continuing until 100 days
dose. May impair fertility in both females (heart, kidney, or pancreas trans-
and males. Children: Safety and efficacy plant) or 200 days (kidney transplant)
not established in pts younger than 1 post-transplant. CHILDREN 1 MO–16
month. Elderly: Age-related renal im- YRS: Once daily based on body surface
pairment may require dosage adjustment. area (BSA) and CrCl using formula:
(Dose = 7 × BSA × CrCl). Maximum:
INTERACTIONS 900 mg/day.
DRUG: Bone marrow depressants may
increase myelosuppression. May increase Dosage in Renal Impairment
concentration/effect of didanosine, my- Dosage and frequency are modified
cophenolate. Probenecid may decrease based on creatinine clearance.
renal clearance, increase concentration. Creatinine Induction Maintenance
May increase nephrotoxic effect of am- Clearance Dosage Dosage
photericin, cycloSPORINE. May increase 60 mL/min 900 mg 900 mg once
adverse effects of zidovudine. Zidovu- or higher twice daily daily
dine (AZT) may increase risk of hema- 40–59 mL/min 450 mg 450 mg once
twice daily daily
tologic toxicity. HERBAL: None significant. 25–39 mL/min 450 mg 450 mg every
FOOD: All foods maximize drug bioavail- once daily 2 days
ability. LAB VALUES: May decrease creati- 10–24 mL/min 450 mg every 450 mg
nine clearance, platelet count, neutrophils, 2 days twice wkly
Hgb, Hct. May increase serum creatinine.
AVAILABILITY (Rx) Dosage in Hepatic Impairment
No dose adjustment.
Powder for Oral Solution: 50 mg/mL
(100 mL). SIDE EFFECTS
Tablets: 450 mg. Frequent (16%–9%): Diarrhea, neutrope-
nia, headache. Occasional (8%–3%): Nau-
ADMINISTRATION/HANDLING sea. Rare (less than 3%): Insomnia,
PO paresthesia, vomiting, abdominal pain,
• Take with meals. • Do not break, fever.
crush, dissolve, or divide tablets; give whole
(potential carcinogen). • Avoid contact ADVERSE EFFECTS/TOXIC
with skin. • Wash skin with soap, water if REACTIONS
contact occurs. • Store oral suspension Hematologic toxicity, including severe neu-
in refrigerator. Discard after 49 days. tropenia (most common), anemia, throm-
V
bocytopenia, leukopenia, aplastic anemia,
INDICATIONS/ROUTES/DOSAGE pancytopenia, bone marrow suppression
Note: Do not use if absolute neutrophil may occur. Retinal detachment occurs
count (ANC) less than 500 cells/mm3, rarely. Overdose may result in renal toxicity.
platelets less than 25,000 cells/mm3, or May decrease sperm production, fertility.
Hgb less than 8 g/dL.
NURSING CONSIDERATIONS
Cytomegalovirus (CMV) Retinitis (AIDS-
Related) BASELINE ASSESSMENT
PO: ADULTS: Initially, 900 mg (two 450- Obtain baseline CBC, serum chemistries,
mg tablets) twice daily for 14–21 days. renal function, urinalysis; pregnancy test.
Maintenance: 900 mg once daily. Receive full medication history.

Canadian trade name Non-Crushable Drug High Alert drug


1192 valproic acid
INTERVENTION/EVALUATION zures. Additional uses for Depakote,
Monitor I&O, ensure adequate hydration Depakote ER: Treatment of manic epi-
(minimum 1,500 mL/24 hrs). Diligently sodes with bipolar disorder, prophylaxis
evaluate CBC for decreased WBCs, Hgb, Hct, of migraine headaches. OFF-LABEL: Refrac-
platelets; changes in urinary characteristics, tory status epilepticus, diabetic neuropathy.
consistency. Question pt regarding vision, Mood stabilizer for behaviors in dementia.
therapeutic improvement, complications.
PRECAUTIONS
PATIENT/FAMILY TEACHING
Contraindications: Hypersensitivity to val-­
• ValGANciclovir provides suppression, p­roic acid. Active hepatic disease, urea cy-
not cure, of CMV retinitis. • Frequent cle disorders, known mitochondrial dis-
blood tests are necessary during therapy orders caused by mutation in mitochon-
because of toxic nature of drug. • Oph- drial DNA polymerase gamma (POLG).
thalmologic exam q4–6wks during treat- Children under 2 yrs of age suspected of
ment is advised. • Report any new symp- having POLG-related disorder. Migraine
tom promptly. • May temporarily or prevention in pregnant women. Cau-
permanently inhibit sperm production in tions: Children younger than 2 yrs. Pts at
men, suppress fertility in women. • Bar- risk for hepatotoxicity. History of hepatic
rier contraception should be used during impairment, bleeding abnormalities, pts
and for 90 days after therapy (mutagenic at high risk for suicide, elderly pts.
potential). • Swallow whole; do not
chew, crush, dissolve, or divide. • Avoid ACTION
handling broken/crushed tablets, oral so- Directly increases concentration of in-
lution. • Report fever, chills, unusual hibitory neurotransmitter gamma-ami-
bleeding/bruising, urinary changes. nobutyric acid (GABA). Therapeutic
Effect: Decreases seizure activity, stabi-
valproic acid lizes mood, prevents migraine headache.
PHARMACOKINETICS
val-pro-ick as-id Well absorbed from GI tract. Protein bind-
(Apo-Divalproex , Depacon, Depak- ing: 80%–90%. Metabolized in liver. Pri-
ene, Depakote, Depakote ER, Depakote marily excreted in urine. Not removed by
Sprinkle, Novo-Divalproex ) hemodialysis. Half-life: 9–16 hrs (may
j BLACK BOX ALERT j Embryo, be increased in hepatic impairment, el-
fetal neural tube defects (spina bi-
fida) have occurred. Life-threaten- derly pts, children younger than 18 mos).
ing pancreatitis, complete hepatic
failure have occurred. LIFESPAN CONSIDERATIONS
Do not confuse Depakene with Pregnancy/Lactation: Drug crosses
Depakote. placenta; is distributed in breast milk.
V Children: Increased risk of hepato-
uCLASSIFICATION toxicity in pts younger than 2 yrs. El-
PHARMACOTHERAPEUTIC: Histone derly: No age-related precautions, but
deacetylase inhibitor. CLINICAL: An- lower dosages recommended.
ticonvulsant, antimanic, antimigraine.
INTERACTIONS
DRUG: Cholestyramine, rifAMPin
USES may decrease concentration/effect. May
Monotherapy/adjunctive therapy of com- increase adverse effects of lamoTRIg-
plex partial seizures, simple and complex ine, LORazepam. HERBAL: None
absence seizures. Adjunctive therapy of significant. FOOD: None known. LAB
multiple seizures including absence sei- VALUES: May increase serum LDH,

underlined – top prescribed drug


valproic acid 1193
bilirubin, ALT, AST. Therapeutic serum wkly intervals up to 60 mg/kg/day. Usual
level: 50–100 mcg/mL; toxic serum adult dosage: 1,000–2,500 mg/day.
level: greater than 100 mcg/mL. IV: ADULTS, ELDERLY, CHILDREN: Same daily
dose divided q6h.
AVAILABILITY (Rx)
Capsules: (Depakene): 250 mg. Cap- Manic Episodes
sules, Sprinkle: (Depakote Sprinkle): PO: ADULTS, ELDERLY: Initially, 500–750
125 mg. Injection Solution: ­
(Depacon): mg/day. May increase by 250–500 mg
100 mg/mL. Oral Solution: (Depakene): q1–3days to reach desired clinical effect
250 mg/5 mL. and therapeutic serum concentration.
Tablets, Delayed-Release: (Depakote):
Maximum: 60 mg/kg/day.
125 mg, 250 mg, 500 mg. Tablets, Extended- Prevention of Migraine Headaches
Release: (Depakote ER): 250 mg, 500 mg. PO: (Extended-Release [Depakote
ER]): ADULTS, ELDERLY: Initially, 500 mg
ADMINISTRATION/HANDLING
once daily. May increase up to 1,000 mg
IV once daily.
PO: (Delayed-Release [Depakote]):
Reconstitution • Dilute each single ADULTS, ELDERLY, CHILDREN 16 YRS AND
dose with at least 50 mL D5W, 0.9% NaCl, OLDER: Initially, 250 mg twice daily. May in-
or lactated Ringer’s. crease up to 1,000 mg/day in 2 divided doses.
Rate of administration • Infuse over
60 min at rate of 20 mg/min or less. • Al- Dosage in Renal Impairment
ternatively, single doses of up to 45 mg/kg No dose adjustment.
given over 5–10 min (1.5–6 mg/kg/min).
Storage • Store vials at room temper- Dosage in Hepatic Impairment
ature. • Diluted solutions stable for 24 Mild to moderate impairment: Not
hrs. • Discard unused portion. recommended. Severe impairment:
Contraindicated.
PO
• May give without regard to food. Do not SIDE EFFECTS
mix oral solution with carbonated beverages Frequent: Epilepsy: Abdominal pain,
(may cause mouth/throat irritation). • May irregular menses, diarrhea, transient
sprinkle capsule (Depakote Sprinkle) con- alopecia, indigestion, nausea, vomiting,
tents on applesauce and give immediately tremors, fluctuations in body weight. Ma-
(do not chew sprinkle beads). • Give de- nia (22%–19%): Nausea, drowsiness.
layed-release/extended-release tablets Occasional: Epilepsy: Constipation, diz-
whole. Do not crush, break, open delayed- ziness, drowsiness, headache, skin rash,
release capsule (Stavzor). • Regular-re- unusual excitement, restlessness. Mania
lease and delayed-release formulations usu- (12%–6%): Asthenia, abdominal pain,
ally given in 2–4 divided doses/day. dyspepsia, rash. Rare: Epilepsy: Mood V
Extended-release formulation (Depakote changes, diplopia, nystagmus, spots be-
ER) usually given once daily. fore eyes, unusual bleeding/bruising.
IV COMPATIBILITIES ADVERSE EFFECTS/TOXIC
Cefepime, cefTAZidime. REACTIONS
Hepatotoxicity may occur, particularly in
INDICATIONS/ROUTES/DOSAGE first 6 mos of therapy. May be preceded
Seizures by loss of seizure control, malaise, weak-
PO: ADULTS, ELDERLY, CHILDREN 10 YRS ness, lethargy, anorexia, vomiting rather
AND OLDER: Initially, 10–15 mg/kg/ than abnormal LFT results. Blood dyscra-
day. May increase by 5–10 mg/kg/day at sias may occur.

Canadian trade name Non-Crushable Drug High Alert drug


1194 valsartan

NURSING CONSIDERATIONS valsartan


BASELINE ASSESSMENT
Anticonvulsant: Review history of sei- val-sar-tan
zure disorder (intensity, frequency, du- (Apo-Valsartan , Diovan)
ration, level of consciousness). Initiate j BLACK BOX ALERT jMay
cause fetal injury, mortality. Dis-
safety measures, quiet dark environment. continue as soon as possible once
CBC should be performed before and 2 pregnancy is detected.
wks after therapy begins, then 2 wks fol- Do not confuse Diovan with
lowing maintenance dose. Obtain base- ­Zyban, or valsartan with
line LFT. Antimanic: Assess behavior, ­losartan or Valstar.
appearance, emotional status, response
to environment, speech pattern, thought FIXED-COMBINATION(S)
content. Antimigraine: Question pt re- Diovan HCT: valsartan/hydroCHLO-
garding onset, location, duration of mi- ROthiazide (a diuretic): 80 mg/12.5
graine, possible precipitating symptoms. mg, 160 mg/12.5 mg, 160 mg/25
INTERVENTION/EVALUATION mg, 320 mg/12.5 mg, 320 mg/25
Monitor CBC, LFT, serum ammonia. An- mg. Byvalson: valsartan/nebivolol
ticonvulsant: Observe frequently for re- (a beta blocker): 80 mg/5 mg. Ex-
currence of seizure activity. Assess skin for forge: valsartan/amLODIPine (a
ecchymoses, petechiae. Monitor for clini- calcium channel blocker): 160 mg/5
cal improvement (decrease in intensity/ mg, 160 mg/10 mg, 320 mg/5 mg,
frequency of seizures). Antimanic: Ques- 320 mg/10 mg. Exforge HCT: val-
tion for suicidal ideation. Assess for thera- sartan/amLODIPine (a calcium chan-
peutic response (interest in surroundings, nel blocker)/hydroCHLOROthiazide
increased ability to concentrate, relaxed (a diuretic): 160 mg/5 mg/12.5 mg,
facial expression). Antimigraine: Evalu- 160 mg/5 mg/25 mg, 160 mg/10
ate for relief of migraine headache and mg/12.5 mg, 160 mg/10 mg/25 mg,
resulting photophobia, phonophobia, 320 mg/10 mg/25 mg. Valturna:
nausea, vomiting. Therapeutic serum valsartan/aliskiren (a direct renin
level: 50–100 mcg/mL; toxic serum inhibitor): 160 mg/150 mg, 320
level: greater than 100 mcg/mL. mg/300 mg.

PATIENT/ FAMILY TEACHING uCLASSIFICATION


• Do not abruptly discontinue medica- PHARMACOTHERAPEUTIC: Angio-
tion after long-term use (may precipitate tensin II receptor antagonist. CLINI-
seizures). • Strict maintenance of drug CAL: Antihypertensive.
therapy is essential for seizure con-
V trol. • Avoid tasks that require alertness, USES
motor skills until response to drug is es-
tablished. • Drowsiness usually disap- Treatment of hypertension alone or in
pears during continued therapy. • Avoid combination with other antihypertensives.
alcohol. • Report liver problems such as Treatment of HF (NYHA Class II–IV). Re-
nausea, vomiting, lethargy, altered mental duce mortality in high-risk pts (left ven-
status, weakness, loss of appetite, abdomi- tricular failure/dysfunction) following MI.
nal pain, yellowing of skin, unusual bruis- PRECAUTIONS
ing/bleeding. • Report if seizure control
worsens, suicidal ideation (depression, Contraindications: Hypersensitivity to val­
unusual changes in behavior, suicidal sartan. Concomitant use with aliskiren in
thoughts) occurs. pts with diabetes. Cautions: Concurrent use
of potassium-sparing diuretics or potas-
underlined – top prescribed drug
valsartan 1195
sium supplements, mild to severe hepatic ADMINISTRATION/HANDLING
impairment, unstented bilateral/unilateral PO
renal artery stenosis, renal impairment, sig- • Give without regard to food.
nificant aortic/mitral stenosis, elderly pts.
INDICATIONS/ROUTES/DOSAGE
ACTION
Hypertension
Directly antagonizes angiotensin II re- PO: ADULTS, ELDERLY: Initially, 80–160
ceptors. Blocks vasoconstrictor, aldo- mg/day in pts who are not volume de-
sterone-secreting effects of angiotensin pleted. Maximum: 320 mg/day. CHIL-
II, inhibiting binding of angiotensin DREN 6–16 YRS: Initially, 1.3 mg/kg
II to AT1 receptors. Therapeutic Ef- once daily (Maximum: 40 mg). May
fect: Produces vasodilation, decreases increase up to 2.7 mg/kg once daily
peripheral resistance, decreases B/P. (Maximum: 160 mg/day).
PHARMACOKINETICS HF
Poorly absorbed after PO administration. PO: ADULTS, ELDERLY: Initially, 20–40
Food decreases peak plasma concentra- mg twice daily. May increase up to 160
tion. Protein binding: 95%. Metabolized mg twice daily. Maximum: 320 mg/day.
in liver. Excreted in feces (83%), urine
(13%). Unknown if removed by hemodi- Post-MI, Left Ventricular Dysfunction
alysis. Half-life: 6 hrs. PO: ADULTS, ELDERLY: May initiate 12
hrs or longer following MI. Initially, 20
LIFESPAN CONSIDERATIONS mg twice daily. May increase within 7 days
Pregnancy/Lactation: May cause fetal to 40 mg twice daily. May further increase
harm. Unknown if distributed in breast up to target dose of 160 mg twice daily.
milk. Children: Safety and efficacy not
established. Elderly: No age-related Dosage in Renal Impairment
precautions noted. CrCl greater than 30 mL/min: No dose
adjustment. CrCl 30 mL/min or less:
INTERACTIONS ADU­LTS: Safety/efficacy not established.
CHILDREN 6–16 YRS: Not recommended.
DRUG: Potassium-sparing drugs (e.g.,
spironolactone, triamterene), potas- Dosage in Hepatic Impairment
sium supplements may increase serum No dose adjustment.
potassium. Aliskiren may increase hyper-
kalemic effect. May increase adverse/toxic- SIDE EFFECTS
ity of ACE inhibitors (e.g., benazepril, Rare (2%–1%): Insomnia, fatigue, heart-
lisinopril). HERBAL: Herbals with hy- burn, abdominal pain, dizziness, head-
pertensive properties (e.g., licorice, ache, diarrhea, nausea, vomiting, arthral-
yohimbe) or hypotensive properties gia, edema.
(e.g., garlic, ginger, ginkgo biloba) V
may alter effects. FOOD: None known. LAB ADVERSE EFFECTS/TOXIC
VALUES: May increase serum bilirubin, ALT, REACTIONS
AST, BUN, creatinine, potassium. May de- Overdosage may manifest as hypotension,
crease Hgb, Hct, WBC. tachycardia. Bradycardia occurs less of-
AVAILABILITY (Rx) ten. Viral infection, upper respiratory
tract infection (cough, pharyngitis, sinus-
Tablets: 40 mg, 80 mg, 160 mg, 320 mg. itis, rhinitis) occur rarely.

Canadian trade name Non-Crushable Drug High Alert drug


1196 vancomycin

NURSING CONSIDERATIONS USES


Systemic: Treatment of infections
BASELINE ASSESSMENT caused by staphylococcal, streptococ-
Obtain CBC, BMP, LFT. Obtain B/P, cal spp. bacteria. PO: Treatment of
apical pulse immediately before each C. difficile–associated diarrhea and
dose, in addition to regular monitoring treatment of enterocolitis caused by
(be alert to fluctuations). If excessive S. aureus (including MRSA). OFF-
reduction in B/P occurs, place pt in LABEL: Treatment of infections caused
supine position, feet slightly elevated. by gram-positive organisms in pts with
Question for possibility of pregnancy. serious allergies to beta-lactam antibiot-
Assess medication history (esp. di- ics; treatment of beta-lactam–resistant
uretic). Question for history of hepatic/ gram-positive infections. Surgical pro-
renal impairment, renal artery stenosis, phylaxis, treatment of prosthetic joint
history of severe HF. infection.
INTERVENTION/EVALUATION PRECAUTIONS
Maintain hydration (offer fluids fre- Contraindications: Hypersensitivity to vanco­
quently). Assess for evidence of upper mycin. Cautions: Renal impairment; con-
respiratory infection. Monitor serum current therapy with other ototoxic, nephro-
electrolytes, renal function, LFT, Hgb, toxic medications, elderly pts, dehydration.
Hct, urinalysis, B/P, pulse. Observe for
symptoms of hypotension. ACTION
PATIENT/ FAMILY TEACHING Binds to bacterial cell walls, altering cell
• Females of childbearing potential membrane permeability, inhibiting RNA
must use effective contraception during synthesis. Therapeutic Effect: Bacte-
treatment. • Inform physician as soon ricidal.
as possible if pregnancy occurs. • Re- PHARMACOKINETICS
port any sign of infection (sore throat,
fever). • Do not stop taking medica- PO: Poorly absorbed from GI tract.
tion. • Report swelling of extremities, Primarily excreted in feces. Paren-
chest pain, palpitations; decreased urine teral: Widely distributed (except CSF).
output, amber-colored urine, fatigue, yel- Protein binding: 10%–50%. Primarily ex-
lowing of the skin or eyes. creted unchanged in urine. Not removed
by hemodialysis. Half-life: 4–11 hrs
(increased in renal impairment).
LIFESPAN CONSIDERATIONS
vancomycin Pregnancy/Lactation: Drug crosses
van-koe-mye-sin placenta, distributed in breast milk follow-
V ing IV administration. Children: Close
(Vancocin)
Do not confuse vancomycin monitoring of serum levels recommended
with clindamycin, gentamicin, in premature neonates, young infants. El-
derly: Age-related renal impairment may
tobramycin, or Vibramycin.
increase risk of ototoxicity, nephrotoxicity;
uCLASSIFICATION dosage adjustment recommended.
PHARMACOTHERAPEUTIC: Tricy- INTERACTIONS
clic glycopeptide antibiotic. CLINI-
CAL: Antibiotic.
DRUG: May increase concentration/
effects of aminoglycosides (e.g.,

underlined – top prescribed drug


vancomycin 1197
amikacin, gentamicin). Bile acid IV INCOMPATIBILITIES
sequestrants (e.g., cholestyramine) Albumin, amphotericin B complex (Abel-
may decrease therapeutic effect (oral cet, AmBisome, Amphotec), aztreonam
vancomycin). HERBAL: None significant. (Azactam), ceFAZolin (Ancef), cefo-
FOOD: None known. LAB VALUES: May taxime (Claforan), cefOXitin (Mefoxin),
increase BUN. Therapeutic peak se- cefTAZidime (Fortaz), cefTRIAXone (Ro-
rum level: (Not routinely obtained) cephin), cefuroxime (Zinacef), foscarnet
20–40 mcg/mL; therapeutic trough (Foscavir), heparin, nafcillin (Nafcil),
serum level: 10–20 mcg/mL. Toxic piperacillin and tazobactam (Zosyn).
peak serum level: greater than 40 mcg/
mL; toxic trough serum level: greater IV COMPATIBILITIES
than 20 mcg/mL. Amiodarone (Cordarone), calcium glu-
conate, dexmedetomidine (Precedex),
AVAILABILITY (Rx)
dilTIAZem (Cardizem), HYDROmor-
Capsules: (Vancocin): 125 mg, 250 mg. phone (Dilaudid), insulin, LORazepam
Infusion, Premix: (Vancocin HCl): 500 (Ativan), magnesium sulfate, midazolam
mg/100 mL, 750 mg/150 mL, 1 g/200 (Versed), morphine, niCARdipine
mL. Injection, Powder for Reconstitution: (Cardene), potassium chloride, propofol
(Vancocin HCl): 500 mg, 750 mg, 1 g. (Diprivan).
Oral Solution: 25 mg/mL, 50 mg/mL.
Oral Suspension: 50 mg/mL. INDICATIONS/ROUTES/DOSAGE
Note: Initial IV dosing in nonobese pts is
ADMINISTRATION/HANDLING
based on actual body weight. Subsequent
IV dosing is adjusted based on serum trough
concentrations and renal function. Pt-­
b ALERT c Give by intermittent IV infu- specific dosing may be necessary to deter-
sion (piggyback) or continuous IV infu- mine dose and interval (e.g., morbid obe-
sion. Do not give IV push (may result in sity, critical illness, unstable renal function).
exaggerated hypotension or red man
syndrome). Usual Parenteral Dosage
Reconstitution • For intermittent IV IV: ADULTS, ELDERLY: 15–20 mg/kg/dose
infusion (piggyback), reconstitute each (rounded to nearest 250 mg) q8–12h.
500-mg vial with 10 mL Sterile Water for Dosage requires adjustment in renal im-
Injection (20 mL for 1-g vial) to provide pairment. Usual Maximum Dose: 2 g.
concentration of 50 mg/mL. • Further CHILDREN OLDER THAN 1 MO: 10–15 mg/kg/
dilute with D5W or 0.9% NaCl to final dose q6h. Maximum: 2,000 mg/dose. NEO-
concentration not to exceed 5 mg/mL. NATES: Loading dose of 20 mg/kg; then, 15
Rate of administration • Administer mg/kg q48h up to 10–15 mg/kg/dose q6–8h.
over 60 min or longer (30 min for each
500 mg recommended). • Monitor B/P Staphylococcal Enterocolitis, Antibiotic- V
closely during IV infusion. Associated Pseudomembranous Colitis
Storage • Reconstituted vials are stable Caused by Clostridium Difficile
for 14 days at room temperature or if refrig- PO: ADULTS, ELDERLY: 125–500 mg 4
erated. • Diluted solutions are stable for 14 times/day for 10–14 days. CHILDREN: 40
days if refrigerated or 7 days at room tem- mg/kg/day in 3–4 divided doses for 7–10
perature. • Discard if precipitate forms. days. Maximum: 2 g/day.
PO Dosage in Renal Impairment
• May give with food. • Powder for After loading dose, subsequent dosages
injection may be reconstituted and di- and frequency are modified based on
luted for oral administration. creatinine clearance, severity of infec-
tion, and serum concentration of drug.
Canadian trade name Non-Crushable Drug High Alert drug
1198 vandetanib
Dosage in Hepatic Impairment
PATIENT/ FAMILY TEACHING
No dose adjustment.
• Continue therapy for full length of
SIDE EFFECTS treatment. • Doses should be evenly
Frequent: PO: Bitter/unpleasant taste, spaced. • Report ringing in ears, hear-
nausea, vomiting, mouth irritation (with ing loss, changes in urinary frequency or
oral solution). Rare: Parenteral: Phle- consistency. • Lab tests are important
bitis, thrombophlebitis, pain at periph- part of total therapy.
eral IV site, dizziness, vertigo, tinnitus,
chills, fever, rash, necrosis with extrava-
sation. PO: Rash. vandetanib
ADVERSE EFFECTS/TOXIC van-det-a-nib
REACTIONS (Caprelsa)
Nephrotoxicity (acute kidney injury, acute j BLACK BOX ALERT jCan pro-
long QT interval (torsades de pointes
tubular necrosis, renal failure), ototoxicity and sudden cardiac death reported).
(temporary or permanent hearing loss) Do not use in pts with hypokalemia,
may occur. Too-rapid infusion may cause hypocalcemia, hypomagnesemia,
red man syndrome, a common adverse congenital long QT syndrome.
reaction characterized by pruritus, urti- Electrolyte imbalances must be
corrected prior to initiating therapy. If
caria, erythema, angioedema, tachycardia, medication that prolongs QT interval
hypotension, myalgia, maculopapular rash is needed, more frequent ECG moni-
(usually appears on face, neck, upper toring is recommended. ECGs should
torso). Cardiovascular toxicity (cardiac de- be obtained during wks 2–4 and wks
pression, arrest) occurs rarely. Onset usu- 8–12 after starting therapy and 3 mos
thereafter. Any dose reduction or
ally occurs within 30 min of start of infu- interruption related to QT prolonga-
sion, resolves within hrs following infusion. tion greater than 2 wks must have
May result from too-rapid rate of infusion. frequent ECG monitoring as noted
above. Only certified prescribers and
NURSING CONSIDERATIONS pharmacies with a restricted distri-
bution program are able to prescribe
BASELINE ASSESSMENT and dispense.
Avoid other ototoxic, nephrotoxic medi-
uCLASSIFICATION
cations if possible. Obtain culture, sensi-
tivity test before giving first dose (therapy PHARMACOTHERAPEUTIC: Epidermal
may begin before results are known). growth factor receptor (EGFR) inhibi-
Consider placement of central venous tor. Vascular endothelial growth factor
line/PICC line. (VEGF) inhibitor. Tyrosine kinase in-
hibitor. CLINICAL: Antineoplastic.
INTERVENTION/EVALUATION
V Monitor serum renal function tests, I&O. As-
sess skin for rash. Check hearing acuity, bal- USES
ance. Monitor B/P carefully during infusion. Treatment of symptomatic or progressive
Monitor for red man syndrome. Evaluate IV medullary thyroid cancer in pts with un-
site for phlebitis (heat, pain, red streaking resectable locally advanced or metastatic
over vein). Obtain vancomycin peak/trough disease.
level as ordered by physician or pharmacist.
Therapeutic serum level: peak: 20–40 PRECAUTIONS
mcg/mL; trough: 10–20 mcg/mL. Toxic Contraindications:Hypersensitivity to
serum level: peak: greater than 40 mcg/ vandetanib. Congenital long QT syn-
mL; trough: greater than 20 mcg/mL. drome. Cautions: Pregnancy, concurrent
medications that prolong QT interval,
underlined – top prescribed drug
vandetanib 1199
hypokalemia, hypomagnesemia, hypothy- AVAILABILITY (Rx)
roidism, cerebrovascular disease, mod- Tablets: 100 mg, 300 mg.
erate to severe renal/hepatic impairment,
hypertension, uncompensated HF, history ADMINISTRATION/HANDLING
of torsades de pointes. PO
• Give without regard to food. • Do
ACTION
not crush. • May disperse in 2 oz of
Inhibits tyrosine kinases including epi- noncarbonated water and stir for 10 min
dermal growth factor (EGF) and vascular until tablet is evenly dispersed (will not
endothelial growth factor (VEGF). Blocks completely dissolve). Administer disper-
intracellular signaling, angiogenesis, and sion immediately. Rinse residue in glass
cellular proliferation. Therapeutic Ef- with 4 oz water and administer. Can be
fect: Inhibits thyroid tumor cell growth given via feeding tube. • Direct contact
and metastasis. of crushed tablets with skin or mu-
cous membranes should be strictly
PHARMACOKINETICS
avoided. If contact occurs, wash thor-
Slowly absorbed following PO adminis- oughly.
tration. Peak concentration: 4–10 hrs. Storage • Contact pharmacy to prop-
Metabolized in liver. Protein binding: erly discard out-of-date tablets.
90%. Excreted in feces (44%), urine
(25%). Half-life: 19 days. INDICATIONS/ROUTES/DOSAGE
Thyroid Cancer
LIFESPAN CONSIDERATIONS
Note: Do not begin unless QTc interval
Pregnancy/Lactation: May cause fetal is less than 450 msec. Maintain se-
harm. Avoid pregnancy. Must use effec- rum calcium and magnesium within nor-
tive contraception during treatment mal limits. Maintain serum potassium at
and for at least 4 mos after treatment. least 4 mEq/L or greater.
Unknown if distributed in breast milk. PO: ADULTS, ELDERLY: 300 mg once
Children: Safety and efficacy not estab- daily. Continue until disease progression
lished. Elderly: No age-related precau- or unacceptable toxicity.
tions noted.
Dosage Adjustment for QT Prolongation
INTERACTIONS or Toxicity
DRUG: Medications prolonging QT Interrupt therapy until resolved or improved,
interval (e.g., amiodarone, azithro- then restart at 100–200 mg once daily.
mycin, citalopram, clarithromycin,
dronedarone, haloperidol, levo- Dosage in Renal Impairment
FLOXacin, quetiapine) may increase CrCl less than 50 mL/min: 200 mg
risk of QT prolongation. CYP3A4 once daily. Closely monitor QT interval.
inducers (e.g., carBAMazepine, V
OXcarbazepine, phenytoin, ri- Dosage in Hepatic Impairment
fAMPin) may decrease concentra- Mild impairment: No dose adjustment.
tion/effects. HERBAL: St. John’s wort Moderate to severe impairment: Not
may decrease concentration/effect. recommended.
FOOD: Grapefruit products may in-
SIDE EFFECTS
crease risk of torsades de pointes, my-
elotoxicity. LAB VALUES: May decrease Frequent (57%–21%): Diarrhea/colitis, rash,
WBC, Hgb, neutrophils. May increase dermatitis acneiform/acne, nausea, head-
serum bilirubin, ALT, AST, creatinine; ache, fatigue, anorexia, abdominal pain.
urine protein. May alter serum calcium, Occasional (15%–10%): Dry skin, vomiting,
glucose, magnesium, potassium. asthenia, photosensitivity, insomnia, na-

Canadian trade name Non-Crushable Drug High Alert drug


1200 varenicline
sopharyngitis, dyspepsia, cough, pruritus, syndrome should be considered in pts
weight decrease, depression. with seizures, headache, visual distur-
bances, confusion, altered mental status.
ADVERSE EFFECTS/TOXIC Ophthalmologic exams including slit
REACTIONS lamp recommended in pts with visual
Prolonged QT interval resulting in tor- disturbances.
sades de pointes, ventricular arrhyth-
mias, sudden cardiac death have been PATIENT/FAMILY TEACHING
reported. Frequent diarrhea may result • Blood levels, ECGs will be routinely
in electrolyte imbalances. Severe skin monitored. • Strictly avoid pregnancy.
reactions, including Stevens-Johnson Contraception should be taken during
syndrome, have been reported. Intersti- treatment and 4 mos after discontinua-
tial lung disease (ILD) or pneumonitis tion. • Changes in mental status, seizures,
reported (may result in respiratory- headache, blurry vision, trouble speaking,
related death). Consider ILD in pts with one-sided weakness may indicate stroke,
hypoxia, pleural effusion, cough, dys- high blood pressure crisis, or life-threaten-
pnea. Ischemic cerebrovascular events ing brain swelling. Immediately report any
have been reported. Life-threatening newly prescribed medications. • Do not
events including hypertensive crisis, take herbal products. • Limit exposure to
reversible posterior leukoencephalopa- sunlight. • Report any yellowing of skin
thy syndrome (RPLS) have been noted. or eyes, abdominal pain, bruising, black/
Adverse reactions resulting in death in- tarry stools, dark urine, decreased urine
cluded respiratory failure/arrest, aspira- output, skin changes. • Report palpita-
tion pneumonia, cardiac failure, sepsis, tions, chest pain, shortness of breath, dizzi-
GI bleeding. ness, fainting (may indicate arrhythmia).

NURSING CONSIDERATIONS
BASELINE ASSESSMENT varenicline
Obtain CBC with differential, serum var-en-i-kleen
chemistries, magnesium, ionized cal- (Champix , Chantix)
cium, TSH, UA, ECG, vital signs. Obtain
negative urine pregnancy before therapy. j BLACK BOX ALERT jRisk of
psychiatric symptoms and suicidal
Question for history of congenital long behavior. Agitation, hostility, de-
QT syndrome, HF, arrhythmias, hepatic/ pressed mood have been reported.
renal impairment, seizures, CVA, hemor-
rhagic events, HTN. Obtain full medica- uCLASSIFICATION
tion history including contraception. PHARMACOTHERAPEUTIC: Selec-
Perform full head-to-toe exam including tive partial nicotine agonist. CLINI-
visual acuity, thorough skin assessment. CAL: Smoking deterrent.
V
INTERVENTION/EVALUATION
Monitor blood levels including electro- USES
lytes esp. during episodes of diarrhea. Aid to smoking-cessation treatment.
Obtain ECG during wks 2–4, wks 8–12,
then every 3 mos thereafter. Obtain ECG PRECAUTIONS
for palpitations, chest pain, hypokalemia, Contraindications: Hypersensitivity to va-
hyperkalemia, hypocalcemia, bradycar- renicline. Cautions: Renal impairment,
dia, ventricular arrhythmias, syncope. history of suicidal ideation or preexisting
Report any respiratory changes including psychiatric illness, bipolar disorder, de-
dyspnea, cough (may indicate ILD). Re- pression, schizophrenia. History of seizures
versible posterior leukoencephalopathy or factors that lower seizure threshold.
underlined – top prescribed drug
varenicline 1201

ACTION additional 12 wks of treatment to increase


Prevents nicotine stimulation of meso- likelihood of long-term abstinence.
limbic dopamine system associated with
Dosage in Renal Impairment
nicotine addiction. Therapeutic Ef-
CrCl less than 30 mL/min: 0.5 mg once
fect: Decreases desire to smoke.
daily. Maximum: 0.5 mg twice daily.
PHARMACOKINETICS End-stage renal disease, undergo-
ing hemodialysis: Maximum: 0.5 mg
Completely absorbed following PO admin-
once daily.
istration. Absorption unaffected by food,
time-of-day dosing. Peak plasma con- Dosage in Hepatic Impairment
centration: 3–4 hrs. Steady state reached No dose adjustment.
within 4 days. Protein binding: 20%.
Minimal metabolism. Removed by hemo- SIDE EFFECTS
dialysis. Primarily excreted unchanged in Frequent (30%–13%): Nausea, insomnia,
urine. Half-life: 24 hrs. headache, abnormal dreams. Occasional
(8%–5%): Constipation, abdominal discom-
LIFESPAN CONSIDERATIONS fort, fatigue, dry mouth, flatulence, altered
Pregnancy/Lactation: Unknown if dis- taste, dyspepsia, vomiting, anxiety, depres-
tributed in breast milk. Children: Not sion, irritability. Rare (3%–1%): Drowsi-
recommended. Elderly: Age-related renal ness, rash, increased appetite, lethargy,
impairment may require dosage adjustment. nightmares, gastroesophageal reflux dis-
ease, rhinorrhea, agitation, mood swings.
INTERACTIONS
DRUG: Histamine H2 receptor an- ADVERSE EFFECTS/TOXIC
tagonists (e.g., famotidine, raniti- REACTIONS
dine) may increase concentration/ef- Abrupt withdrawal may cause irritability,
fect. May increase concentration/effect sleep disturbances in 3% of pts. Hyperten-
of nicotine HERBAL: None significant. sion, angina pectoris, arrhythmia, bradycar-
FOOD: None known. LAB VALUES: None dia, coronary artery disease, gingivitis, ane-
significant. mia, lymphadenopathy occur rarely. May
cause bizarre behavior, suicidal ideation.
AVAILABILITY (Rx)
Tablets, Film-Coated: 0.5 mg, 1 mg. NURSING CONSIDERATIONS
BASELINE ASSESSMENT
ADMINISTRATION/HANDLING
• Give after meal and with full glass of Screen, evaluate for coronary heart dis-
water. • Do not break, crush, dissolve, ease (history of MI, angina pectoris),
or divide film-coated tablets. cardiac arrhythmias, suicidal ideation.
Assess smoking pack/yr history.
INDICATIONS/ROUTES/DOSAGE V
INTERVENTION/EVALUATION
b ALERT c Therapy should start 1 wk
Discontinue use if cardiovascular symp-
before stopping smoking.
toms occur or worsen. Monitor for psy-
Smoking Deterrent chiatric symptoms (changes in behavior,
PO: ADULTS, ELDERLY: Days 1–3: 0.5 mg mood, level of interest, appearance). Assess
once daily.Days 4–7: 0.5 mg twice daily. for cravings, noncompliance with cessation.
Day 8–end of treatment: 1 mg twice daily. PATIENT/FAMILY TEACHING
Therapy should last for total of 12 wks. Pts
• Initiate treatment 1 wk before quit-
who have successfully stopped smoking at
smoking date. • Take with food and
the end of 12 wks should continue with an

Canadian trade name Non-Crushable Drug High Alert drug


1202 vasopressin
with full glass of water. • With twice- tance and mean arterial BP; increases
daily dosing, take 1 tablet in morning, 1 water permeability at renal tubules,
in evening. • Report persistent nausea, causing a decreased urine volume and
insomnia. • Report change in behavior, increased osmolality; causes smooth
mood, level of interest, appearance. muscle contraction in GI tract.
PHARMACOKINETICS
Route Onset Peak Duration
vasopressin IV N/A N/A 0.5–1 hr
IM, SQ 1–2 hrs N/A 2–8 hrs
vay-soe-pres-in
(Pressyn , Pressyn AR , Distributed throughout extracellular
Vasostrict) fluid. Metabolized in liver, kidney. Pri-
Do not confuse Pitressin with marily excreted in urine. Half-life: 10–
Pitocin. 20 min.

uCLASSIFICATION LIFESPAN CONSIDERATIONS


PHARMACOTHERAPEUTIC: Posterior Pregnancy/Lactation: Caution in giving
pituitary hormone. CLINICAL: Vaso- to breastfeeding women. Children/El-
pressor, antidiuretic hormone ana- derly: Caution due to risk of water in-
logue. toxication/hyponatremia.
INTERACTIONS
USES DRUG: None significant. HERBAL: None
Prevention/control of polydipsia, poly- significant. FOOD: None known. LAB
uria, dehydration in pts with neurogenic VAL­UES: None significant.
diabetes insipidus or differential diag-
nosis of diabetes insipidus. Vasocon- AVAILABILITY (Rx)
striction: To increase blood pressure Injection Solution: 20 units/mL.
in adults with vasodilatory shock who
remain hypotensive despite fluids and ADMINISTRATION/HANDLING
catecholamines. OFF-LABEL: Adjunct in IV
treatment of acute massive GI hemor-
rhage or esophageal varices. Reconstitution • Dilute with D5W or
0.9% NaCl to concentration of 0.1–1 unit/
PRECAUTIONS mL (usual concentration: 100 units/­500 mL
Contraindications: Hypersensitivity to vaso­ D5W).
pressin. Cautions: Seizure disorder, mi- Rate of administration • Give as IV
graine, asthma, vascular disease, renal/ infusion.
cardiac disease, goiter (with cardiac Storage • Store at room temperature.
V
complications), arteriosclerosis, nephri-
IM, SQ
tis, elderly pts.
• Give with 1–2 glasses of water to re-
ACTION duce side effects.
Stimulates a family of arginine vasopres- IV INCOMPATIBILITIES
sin (AVP) receptors. Therapeutic Ef-
Furosemide (Lasix), phenytoin (Dilantin).
fect: Increases systemic vascular resis-

underlined – top prescribed drug


vedolizumab 1203

IV COMPATIBILITIES INTERVENTION/EVALUATION
Amiodarone, argatroban, dilTIAZem Monitor I&O closely, restrict intake as
(Cardizem), DOBUTamine (Dobutrex), necessary to prevent water intoxication.
DOPamine (Intropin), heparin, insulin, mil- Weigh daily if indicated. Check B/P, pulse
rinone (Primacor), nitroglycerin, norepi- frequently. Monitor serum electrolytes,
nephrine (Levophed), pantoprazole (Proto- Hgb, Hct, urine specific gravity. Evaluate
nix), phenylephrine (Neo-Synephrine). injection site for erythema, pain, abscess.
Report side effects to physician for dose
INDICATIONS/ROUTES/DOSAGE reduction. Be alert for early signs of wa-
Diabetes Insipidus ter intoxication (drowsiness, listlessness,
Note: May be administered intranasally headache, seizures). Observe for evi-
by nasal spray or on cotton pledgets; dos- dence of GI bleeding. Withhold medica-
age is individualized. tion, report immediately any chest pain,
IM, SQ: ADULTS, ELDERLY: 5–10 units allergic symptoms.
2–4 times/day. CHILDREN: 2.5–10 units, PATIENT/FAMILY TEACHING
2–4 times/day.
• Promptly report headache, chest pain,
Vasodilatory Shock shortness of breath, other symp-
IV infusion: ADULTS, ELDERLY: Initially, toms. • Stress importance of I&O. •
0.03 units/min. Titrate by 0.005 units/ Avoid alcohol. • Report confusion, sei-
min at 10–15-min intervals. Maximum: zure activity.
0.1 units/min.
Dosage in Renal/Hepatic Impairment
No dose adjustment. vedolizumab
SIDE EFFECTS ve-doe-liz-ue-mab
Frequent: Pain at injection site (with va- (Entyvio)
sopressin tannate). Occasional: Abdom- Do not confuse vedolizumab
inal cramps, nausea, vomiting, diarrhea, with certolizumab, eculizumab,
dizziness, diaphoresis, pale skin, circum- natalizumab, omalizumab,
oral pallor, tremors, headache, eructa- tocilizumab.
tion, flatulence. Rare: Chest pain, confu-
sion, allergic reaction (rash, urticaria, uCLASSIFICATION
pruritus, wheezing, difficulty breathing, PHARMACOTHERAPEUTIC: Selective
facial/peripheral edema), sterile abscess adhesion molecule inhibitor. Mono-
(with vasopressin tannate). clonal antibody. CLINICAL: GI agent.
ADVERSE EFFECTS/TOXIC
REACTIONS USES V
Anaphylaxis, MI, water intoxication have Treatment of adult pts with moderately to
occurred. Elderly, very young are at severely active ulcerative colitis (UC) who
higher risk for water intoxication. have had an inadequate response with,
lost response to, or were intolerant to a
NURSING CONSIDERATIONS tumor necrosis factor (TNF) blocker or
BASELINE ASSESSMENT immunomodulator; or had an inadequate
response with, were intolerant to, or dem-
Establish baselines for weight, B/P, pulse, onstrated dependence on corticosteroids.
serum electrolytes, Hgb, Hct, urine spe- Treatment of adult pts with moderately to
cific gravity. severely active Crohn’s disease (CD) who

Canadian trade name Non-Crushable Drug High Alert drug


1204 vedolizumab
have had an inadequate response with, AVAILABILITY (Rx)
lost response to, or were intolerant to a Lyophilized Powder for Injection: 300 mg.
TNF blocker or immunomodulator; or
had an inadequate response with, were ADMINISTRATION/HANDLING
intolerant to, or demonstrated depen- IV
dence on corticosteroids.
• Do not administer IV push or bo-
PRECAUTIONS lus. • Reconstitute with Sterile Water for
Contraindications: Hypersensitivity to Injection and subsequently dilute with 0.9%
vedolizumab. Cautions: Hepatic impair- NaCl only. • After infusion completed,
ment, immunocompromised pts, live flush IV line with 30 mL of 0.9% NaCl.
vaccine administration. Active infections Reconstitution • Remove flip cap
(not recommended during active infec- and swab with alcohol. • Reconstitute
tion), conditions predisposing to infec- vial with 4.8 mL Sterile Water for Injec-
tions (e.g., diabetes, renal failure, open tion. Direct stream toward glass wall to
wounds, indwelling catheters). Preexist- avoid excessive foaming. • Gently swirl
ing or recent-onset CNS demyelinating contents for at least 15 sec until com-
disorders including multiple sclerosis. pletely dissolved. • Do not shake or
invert vial. • Allow solution to sit at
ACTION room temperature for up to 20 min to
Binds to T-lymphocyte integrin receptors allow remaining foam to settle and pow-
and blocks the interaction with mucosal der to dissolve. If not fully dissolved after
addressin cell adhesion molecule-1 (MAd- 20 min, allow additional 10 min for dis-
CAM-1). Inhibits migration and homing of solution. Do not use if product is not
memory T-lymphocytes into inflamed GI dissolved within 30 min. • Visually in-
tissue. Therapeutic Effect: Reduces spect for particulate matter and discolor-
chronic inflammation of colon. ation. Do not use if discolored or if
­particle matter is observed. • Prior to
PHARMACOKINETICS withdrawing solution, invert vial 3 times
Metabolism not specified. Excretion not to ensure mixing. • Withdraw 5 mL and
specified. Half-life: 25 days. further dilute in 250 mL 0.9% NaCl
bag. • Infuse immediately.
LIFESPAN CONSIDERATIONS Rate of administration • Infuse over
Pregnancy/Lactation: Unknown if dis­ 30 min.
tributed in breast milk. Use caution when Storage • Reconstituted solution should
administering to nursing women. Chil- appear clear to opalescent, colorless to
dren: Safety and efficacy not established. light brownish yellow and free of parti-
Elderly: No age-related precautions noted. cles. • May refrigerate diluted solution for
up to 4 hrs.
V INTERACTIONS
INDICATIONS/ROUTES/DOSAGE
DRUG: Anti-TNF agents (e.g., adali-
mumab, certolizumab, etanercept, Ulcerative Colitis and Crohn’s Disease
infliximab) may increase adverse IV: ADULTS, ELDERLY: 300 mg once at
effects. May decrease the therapeu- wk 0, wk 2, and wk 6, then every 8 wks
tic effect; increase adverse effects of thereafter. Discontinue in pts who do not
vaccines (live). HERBAL: Echinacea show evidence of therapeutic benefit by
may decrease the therapeutic effect. wk 14.
FOOD: None known. LAB VALUES: May
Dosage in Renal Impairment
increase serum ALT, AST, bilirubin. Use caution.

underlined – top prescribed drug


vedolizumab 1205
Dosage in Hepatic Impairment mm or greater with tuberculin skin test
Use caution. Discontinue for jaundice or should be considered a positive result
signs/symptoms of hepatic injury. when assessing for latent TB. Antifun-
gal therapy should be considered for
SIDE EFFECTS those who reside in or travel to regions
Occasional (13%–4%): Nasopharyngitis, where mycoses are endemic. Have
headache, arthralgia, nausea, pyrexia, supplemental oxygen, anaphylaxis kit
upper respiratory tract infection, fa- readily available. Conduct full neuro-
tigue, cough, bronchitis, influenza, back logic exam. Question history of malig-
pain. Rare (3%): Rash, pruritus, sinus- nancies.
itis, oropharyngeal pain, extremity pain.
INTERVENTION/EVALUATION
ADVERSE EFFECTS/TOXIC Routinely monitor LFT. Withhold treat-
REACTIONS ment if acute infection, opportunistic
Infusion-related reactions, including infection, sepsis occurs and initiate
anaphylaxis, characterized by broncho- appropriate antimicrobial therapy.
spasm, dyspnea, flushing, hypotension, Monitor for hypersensitivity reaction.
laryngeal edema, nausea, pyrexia, tachy- Infusion-related reactions generally oc-
cardia, wheezing, vomiting, reported in cur within 2 hrs after infusion. Consider
less than 1% of pts. May increase risk of administration of antihistamine, anti-
severe infections such as anal abscess, pyretic, and/or corticosteroid if mild
cytomegaloviral colitis, giardiasis, Liste- to moderate hypersensitivity reaction
ria meningitis, Salmonella sepsis, TB, occurs. If anaphylaxis occurs, provide
UTI, which may lead to fatal sepsis. PML immediate resuscitation support. Moni-
(weakness, paralysis, vision loss, apha- tor for new onset or worsening of neu-
sia, cognition impairment) has occurred rologic symptoms, esp. in pts with CNS
rarely; however, immunocompromised disorders; may indicate PML.
pts are at increased risk for development. PATIENT/FAMILY TEACHING
Drug-induced hepatotoxicity with serum
ALT, AST greater than 3 times upper limit • Blood levels, TB screening will be
of normal reported in less than 2% of pts. routinely monitored. • Therapy may
Malignancies including B-cell lymphoma, lower immune system response. Report
breast cancer, colon cancer, lung cancer travel plans to possible endemic ar-
of primary neuroendocrine carcinoma, eas. • Do not receive live vaccines un-
lung neoplasm, malignant hepatic neo- less approved by your doctor. • Report
plasm, melanoma, renal cancer, squa- history of fungal infections, multiple scle-
mous cell carcinoma, transitional cell rosis, TB or close relatives who have ac-
carcinoma occur rarely. Immunogenicity tive TB. • Infusion may cause severe
(anti-vedolizumab antibodies) occurred allergic reactions such as face/tongue
in 4%–13% of pts. swelling, hives, itching, low blood pres- V
sure, trouble breathing, or, in some
NURSING CONSIDERATIONS cases, anaphylaxis. • Do not breast-
feed. • Abdominal pain, bruising, clay-
BASELINE ASSESSMENT colored stools, dark-amber urine, fa-
Obtain CBC, LFT. Prior to initiating tigue, loss of appetite, yellowing of skin
treatment, all pts should be up to date or eyes may indicate liver prob-
with all immunizations according to lem. • Paralysis, vision changes, im-
proper guidelines. Continuously screen paired speech, altered mental status may
for active infection. Evaluate for active indicate life-threatening neurologic event
TB and test for latent infection prior to called progressive multifocal leukoen-
and during treatment. Induration of 5 cephalopathy (PML).

Canadian trade name Non-Crushable Drug High Alert drug


1206 vemurafenib

INTERACTIONS
vemurafenib DRUG: Strong CYP3A4 inhibitors
(e.g., clarithromycin, ketoconazole)
vem-ue-raf-e-nib
may increase concentration/effect. Strong
(Zelboraf)
CYP3A4 inducers (e.g., carBAMaze-
uCLASSIFICATION pine, phenytoin, rifAMPin) may de-
crease concentration/effect. May increase
PHARMACOTHERAPEUTIC: BRAF
concentration/effect of digoxin. Medica-
kinase inhibitor. CLINICAL: Antineo-
tions that prolong QT interval (e.g.,
plastic.
amiodarone, azithromycin, clarithro-
mycin, haloperidol, moxifloxacin) may
USES increase risk of QT interval prolongation.
Treatment of unresectable or metastatic May increase bleeding effect with warfarin.
HERBAL: St. John’s wort may decrease
melanoma with a BRAF V600E mutation
as detected by FDA-approved test. Treat- concentration/effect. FOOD: None known.
LAB VALUES: May increase serum alkaline
ment of Erdheim-Chester disease (ECD)
in pts with a BRAF V600E mutation. phosphatase, ALT, AST, gamma-glutamyl
transferase (GGT), bilirubin.
PRECAUTIONS
AVAILABILITY (Rx)
Contraindications: Hypersensitivity to ve-
murafenib. Cautions: Avoid sun exposure. Film-Coated Tablets: 240 mg.
Prior radiation therapy. Prolonged QT syn-
drome, concurrent use of medications that ADMINISTRATION/HANDLING
prolong QT interval, hepatic impairment, PO
uncorrected electrolyte imbalance (hypo- • Give in morning and evening approxi-
kalemia, hypomagnesemia), elderly pts. mately 12 hrs apart. • Give without re-
gard to food. • Do not break, crush,
ACTION dissolve, or divide tablets; swallow
Inhibits kinase activity of certain mu- whole. • Give with full glass of water.
tated forms of BRAF. Therapeutic Ef-
fect: Blocks tumor cell proliferation in INDICATIONS/ROUTES/DOSAGE
melanoma with the mutation. Note: Management of adverse drug
reactions may require dose reduction,
PHARMACOKINETICS treatment interruption, or discontinua-
Readily absorbed after PO administra- tion.
tion. Protein binding: 99%. Minimally
ECD, Melanoma
metabolized in liver. Primarily excreted
in feces (94%). Half-life: 57 hrs. PO: ADULTS, ELDERLY: 960 mg twice
Range: 30–120 hrs. daily (in morning and evening about 12
V hrs apart). Continue until disease pro-
LIFESPAN CONSIDERATIONS gression or unacceptable toxicity.
Pregnancy/Lactation: Avoid pregnancy. Dosage Modification
May cause fetal harm. Must use effective Based on Common Terminology Criteria
contraception during treatment and for at for Adverse Events (CTCAE). Grade 1 or
least 2 mos after discontinuation. Unknown Grade 2 (tolerable): No dose adjustment.
if distributed in breast milk. Must either Grade 2 (intolerable) or Grade 3: First
discontinue breastfeeding or discontinue incident: Interrupt treatment until toxicity
therapy. Children: Safety and efficacy not returns to Grade 0 or 1, then resume at 720
established. Elderly: May have increased mg twice daily. Second incident: Inter-
risk of adverse reactions, side effects. rupt treatment, then resume at 480 mg
underlined – top prescribed drug
venetoclax 1207
twice daily. Third incident: Discontinue. INTERVENTION/EVALUATION
Grade 4: First incident: Interrupt treat- Monitor ECG 15 days after initiation,
ment, then resume at 480 mg twice daily. then monthly for first 3 mos, then q3mos
Second incident: Discontinue. thereafter. Routinely assess skin and for
6 mos after discontinuation. Immediately
Dosage in Renal/Hepatic Impairment report any new skin lesions. Obtain ECG
Mild to moderate impairment: No for palpitations, chest pain, hypokalemia,
dose adjustment. hyperkalemia, hypocalcemia, bradycar-
Severe impairment: Use with caution. dia, ventricular arrhythmias, syncope.
SIDE EFFECTS Monitor PT/INR while pt is on warfarin.
Pruritus, difficulty breathing, erythema,
Frequent (53%–33%): Arthralgia, alopecia, hypotension may indicate anaphylaxis.
fatigue, rash, nausea. Occasional (28%–
11%): Diarrhea, hyperkeratosis, headache, PATIENT/FAMILY TEACHING
pruritus, pyrexia, dry skin, extremity pain, • Blood levels, ECG, eye examinations are
anorexia, vomiting, peripheral edema, routinely ordered. • Strictly avoid preg-
erythema, dysgeusia, myalgia, constipation, nancy. Contraception should be used dur-
asthenia. Rare (8%–5%): Maculopapular ing treatment and for 2 mos after last
rash, actinic keratosis, musculoskeletal dose. • Avoid sunlight exposure. •
pain, back pain, cough, papular rash. Report any skin changes, including new
warts, sores, reddish bumps that bleed or
ADVERSE EFFECTS/TOXIC do not heal, change in mole size or
REACTIONS color. • Report yellowing of skin or
Cutaneous squamous cell carcinoma eyes, abdominal pain, bruising, black/
(cuSCC) and keratoacanthomas reported tarry stools, dark urine, decreased urine
in 24% of pts. Pts at increased risk of output, skin changes. • Report palpita-
cuSCC include elderly pts, pts with prior tions, chest pain, shortness of breath, diz-
skin cancer, chronic sun exposure. Hyper- ziness, fainting (may indicate arrhythmia).
sensitivity reactions including erythema,
hypotension, anaphylaxis reported. Mild
to severe photosensitivity was reported.
Serious dermatologic reactions include venetoclax
Stevens-Johnson syndrome, toxic epider-
mal necrolysis. Ophthalmologic reactions ven-et-oh-klax
including uveitis reported. Increased LFT (Venclexta)
may lead to discontinuation. Do not confuse venetoclax or
Venclexta with Venelex.
NURSING CONSIDERATIONS
uCLASSIFICATION
BASELINE ASSESSMENT
Confirm presence of BRAF V600E muta- PHARMACOTHERAPEUTIC: B-cell lym- V
tion. Review history for previous radia- phoma-2 inhibitor. CLINICAL: Antine­
tion therapy. Obtain serum chemistries, oplastic.
renal function test, serum magnesium,
ionized calcium, ECG, PT/INR if taking USES
warfarin. Assess skin for moles, lesions,
papilloma, and perform full dermatologic Monotherapy or in combination with
exam. Obtain baseline ophthalmologic rituximab for treatment of pts with
exam, visual acuity. Assess medication chronic lymphocytic leukemia (CLL) or
history for QT-prolonging drugs. Obtain small lymphocytic leukemia (SLL) with or
negative urine pregnancy before initiating without 17p deletion who have received
treatment. Offer emotional support. at least one prior therapy. Treatment

Canadian trade name Non-Crushable Drug High Alert drug


1208 venetoclax
of newly diagnosed acute myeloid leuke- moderate CYP3A inhibitors (e.g.,
mia (AML) (in combination with azaciti- dilTIAZem, fluconazole, verapamil),
dine, decitabine, or low-dose cytarabine) P-gp inhibitors (e.g., cycloSPORINE,
in pts 75 yrs of age or older, or with co- ranolazine, ticagrelor) may increase
morbidities precluding use of intensive concentration/effect. Strong CYP3A
induction chemotherapy. inducers (e.g., carBAMazepine, phe­
nytoin, rifAMPin) may decrease con-
PRECAUTIONS centration/effect. May increase concen-
Contraindications: Hypersensitivity to tration/effect of digoxin. May decrease
venetoclax. Concomitant use of strong the therapeutic effect; increase adverse
CYP3A inhibitors at initiation and during effects of vaccines (live). HERBAL: Bit-
ramp-up phase. Cautions: Baseline ane- ter orange may increase concentration/
mia, leukopenia, neutropenia, thrombo- effect. FOOD: Grapefruit products, Se-
cytopenia; concomitant use of moderate ville oranges, starfruit may increase
CYP3A inhibitors, P-gp inhibitors; active concentration/effect. Low-fat meals,
infection or pts at increased risk of infec- high-fat meals increase exposure/con-
tion (diabetes, kidney failure, indwelling centration. LAB VALUES: May decrease
catheters, open wounds), hepatic/renal Hgb, Hct, neutrophils, platelets, RBCs;
impairment, electrolyte imbalance; his- serum calcium, potassium. Tumor lysis
tory of gout; pts at high risk for tumor syndrome may result in elevated serum
lysis syndrome (high tumor burden). phosphate, potassium, uric acid.
ACTION AVAILABILITY (Rx)
Binds to and inhibits B-cell lymphoma-2 Tablets: 10 mg, 50 mg, 100 mg.
protein and displaces proapoptotic pro-
teins, restoring process of apoptosis. ADMINISTRATION/HANDLING
Therapeutic Effect: Inhibits tumor cell PO
growth and metastasis. • Give with food and water at same time
each day. • Administer tablets whole;
PHARMACOKINETICS do not cut, crush, or divide. • If a dose
Widely distributed. Metabolized in liver. is missed by no more than 8 hrs, admin-
Protein binding: highly bound (unspeci- ister as soon as possible. If dose is
fied). Peak plasma concentration: 5–8 missed by more than 8 hrs or if vomiting
hrs. Excreted in feces (greater than occurs after dosing, skip dose and ad-
99%). Half-life: 26 hrs. minister the next dose on schedule.
LIFESPAN CONSIDERATIONS INDICATIONS/ROUTES/DOSAGE
Pregnancy/Lactation: Avoid pregnancy; CLL
may cause fetal harm/malformations. Fe- PO: ADULTS, ELDERLY: Week 1: 20 mg
V male and male pts of reproductive potential once daily for 7 days. Week 2: 50 mg
should use effective contraception dur- once daily for 7 days. Week 3: 100
ing treatment and for at least 30 days after mg once daily for 7 days. Week 4: 200
discontinuation. Unknown if distributed mg once daily for 7 days. Week 5 and
in breast milk. Breastfeeding not recom- thereafter: 400 mg once daily. Continue
mended. May impair fertility in males. Chil- until disease progression or unacceptable
dren: Safety and efficacy not established. toxicity. In combination with ritux-
Elderly: No age-related precautions noted. imab: Week 5 and thereafter: 400
mg once daily. Continue until disease pro-
INTERACTIONS gression or unacceptable toxicity for up to
DRUG: Strong CYP3A inhibitors (e.g., 24 mos from day 1 (cycle 1) of rituximab.
clarithromycin, ketoconazole), Begin rituximab after receiving venetoclax
underlined – top prescribed drug
venetoclax 1209
at 400 mg once daily for 7 days. In com- Grade 3 or 4 Nonhematologic Toxicity
bination with obinutuzumab: Obinu- First occurrence: Withhold treatment
tuzumab begins on day 1 of cycle 1. Begin until resolved to Grade 1 or baseline,
venetoclax on day 22 of cycle 1 (based then resume at same dose. Second and
on 5-wk ramp-up schedule). Ramp-up is subsequent occurren­ces: Withhold
completed at end of cycle 2. Cycle 3 (day treatment until resolved, then follow dose
1 and beyond): 400 mg once daily until reduction schedule (or reduce dose at pre-
end of cycle 12. Each cycle is 28 days. scriber’s discretion).

AML Hematologic Toxicity


PO: ADULTS 75 YRS OR OLDER: Day 1: 100 First occurrence of Grade 3 or 4
mg once daily. Day 2: 200 mg once daily. neutropenia with infection or fever;
Day 3: 400 mg once daily. In combination Grade 4 hematologic toxicity (ex-
with azaCITIDine or decitabine: Day 4 cept lymphopenia): Withhold treat-
and beyond: 400 mg once daily. Continue ment until resolved to Grade 1 or base-
until disease progression or unacceptable line, then resume at same dose. Second
toxicity. In combination with low-dose and subsequent occurren­ces: With-
cytarabine: Day 4 and beyond: 600 mg hold treatment until resolved, then follow
once daily. Continue until disease progres- dose reduction schedule (or reduce dose
sion or unacceptable toxicity. at prescriber’s discretion).

Dose Modification Concomitant Use CYP3A Inhibitors, P-gp


Based on Common Terminology Criteria for Inhibitors
Adverse Events (CTCAE). For pts with dose Strong CYP3A inhibitors: Avoid in-
interruption greater than 1 wk during 5-wk hibitor or reduce venetoclax dose by at
ramp-up phase or greater than 2 wks at 400 least 75%. Moderate CYP3A inhibitors
mg daily dose, reassess risk of tumor lysis or P-gp Inhibitors: Avoid inhibitor or
syndrome to determine if reinitiation with a reduce venetoclax dose by at least 50%.
reduced dose is needed. Consider discon-
tinuation in pts who require reduced dosage Dosage in Renal/Hepatic Impairment
of less than 100 mg for more than 2 wks. Mild to moderate impairment: No
dose adjustment. Severe impair-
Dose Reduction Schedule ment: Not specified; use caution.
Note: During ramp-up phase, continue re-
duced dose for 1 wk before increasing dose. SIDE EFFECTS
Dose interruption at 400 mg: Resume Frequent (35%–14%): Diarrhea, ­nausea,
at 300 mg. Dose interruption at 300 fatigue, pyrexia, vomiting, headache, con-
mg: Resume at 200 mg. Dose inter- stipation. Occasional (13%–10%): Cough,
ruption at 200 mg: Resume at 100 mg. peripheral edema, back pain.
Dose interruption at 100 mg: Resume
at 50 mg. Dose interruption at 50 ADVERSE EFFECTS/TOXIC V
mg: Resume at 20 mg. Dose interrup- REACTIONS
tion at 20 mg: Resume at 10 mg. Anemia, neutropenia, thrombocytope-
nia are expected responses to therapy.
Tumor Lysis Syndrome
Grade 3 or 4 neutropenia reported in
Any occurrence of blood chemistry
41% of pts. Pts with high tumor bur-
abnormalities: Withhold next dose, then
den, renal impairment, concomitant
resume at same dose if resolved within 24– use of strong or moderate CYP3A in-
48 hrs of last dose. If not resolved within hibitors, P-gp inhibitors may experi-
48 hrs, resume at reduced dose. ence life-threatening tumor lysis syn-
Any event of tumor lysis syndrome:
drome, which mainly occurs during
Resume at reduced dose once resolved. the 5-wk ramp-up phase and as early
Canadian trade name Non-Crushable Drug High Alert drug
1210 venlafaxine
as 6–8 hrs after dose (hospitalization as body aches, chills, cough, fatigue, fever.
may be necessary). Tumor lysis syn- Avoid those with active infection. • Ther-
drome may cause renal failure requir- apy may cause tumor lysis syndrome (a
ing emergent dialysis. Other reactions condition caused by the rapid breakdown
may include upper respiratory tract of cancer cells), which can cause kidney
infection, pneumonia, autoimmune he- failure and may lead to death. Report de-
molytic anemia. creased urination, amber-colored urine,
confusion, difficulty breathing, fatigue, fe-
NURSING CONSIDERATIONS ver, muscle or joint pain, palpitations,
BASELINE ASSESSMENT seizures, vomiting. • Drink at least 6–8
glasses of water every day. • Avoid preg-
Obtain ANC, CBC, BMP, renal function nancy. Female and male pts of childbear-
test; serum phosphate, calcium; vital ing potential should use effective contra-
signs prior to initiation and periodically ception during treatment and for at least
thereafter. Obtain pregnancy test in fe- 30 days after last dose. Do not breast-
male pts of reproductive potential. Ques- feed. • Treatment may impair fertil-
tion history of hepatic/renal impairment, ity. • Avoid grapefruit products, Seville
gout. Assess all pts for high risk of tumor oranges, starfruit, herbal supplements.
lysis syndrome and provide adequate hy- • Do not take newly prescribed medica-
dration and antihyperuricemics (accord- tions unless approved by prescriber who
ing to manufacturer guidelines) prior originally started therapy. • Do not re-
to first dose. Conduct tumor burden as- ceive live vaccines.
sessments including blood chemistries,
radiologic testing (e.g., CT scan). Correct
electrolyte imbalances prior to initiation.
Receive full medication history (esp. venlafaxine
CYP3A inhibitors, P-gp inhibitors, drugs
with narrow therapeutic index). Screen ven-la-fax-een
for active infection. Offer emotional sup- (Effexor XR)
port. j BLACK BOX ALERT jIncreased
risk of suicidal ideation and behavior
INTERVENTION/EVALUATION in children, adolescents, young adults
Monitor ANC, CBC for anemia, leukope- 18–24 yrs with major depressive
nia, neutropenia, thrombocytopenia. Dil- disorder, other psychiatric disorders.
igently monitor for tumor lysis syndrome uCLASSIFICATION
(acute renal failure, electrolyte imbal-
ance, cardiac arrhythmias, seizures). PHARMACOTHERAPEUTIC: Seroto-
Monitor for infection and provide appro- nin-norepinephrine reuptake inhibi-
priate antimicrobial therapy if indicated. tor (SNRI). CLINICAL: Antidepressant.
To reduce risk of neutropenia-associated
V infection, consider administration of USES
granulocyte-colony stimulating factor
(e.g., filgrastim). Monitor for toxicities if Treatment of depression. Treatment of
discontinuation of CYP3A inhibitors, P-gp generalized anxiety disorder (GAD),
inhibitors is unavoidable. Monitor I&O. social anxiety disorder (SAD). Treat-
Assess hydration status. ment of panic disorder, with or without
agoraphobia. OFF-LABEL: Treatment of
PATIENT/FAMILY TEACHING attention-deficit hyperactivity disorder
• Treatment may depress your immune (ADHD), obsessive-compulsive disorder
system and reduce your ability to fight in- (OCD), hot flashes, diabetic neuropathy,
fection. Report symptoms of infection such post-traumatic stress disorder (PTSD).

underlined – top prescribed drug


venlafaxine 1211

PRECAUTIONS NSAIDs (e.g., ibuprofen, ketoro-


Contraindications: Hypersensitivity to ven­ lac, naproxen), as­ pirin, warfarin.
lafaxine. Use of MAOIs intended to treat HERBAL: St. John’s wort may decrease
psychiatric disorders concurrently or concentration/effect. Herbals with an-
within 14 days of discontinuing MAOI. ticoagulant/antiplatelet properties
Initiation of MAOI to treat psychiatric (e.g., garlic, ginger, ginkgo biloba),
disorder within 7 days of discontinuing glucosamine may increase risk of bleed-
venlafaxine, initiation in pts receiving line- ing. FOOD: Grapefruit products may
zolid or IV methylene blue. Cautions: Sei- increase concentration/effect. LAB VAL-
zure disorder, renal/hepatic impairment, UES: May increase serum cholesterol CPK,
pts at high risk for suicide, recent MI, ma- LDH, prolactin, GGT.
nia, volume-depleted pts, narrow-angle
AVAILABILITY (Rx)
glaucoma, HF, hyperthyroidism, abnormal
platelet function, elderly pts. Tablets: 25 mg, 37.5 mg, 50 mg, 75 mg,
100 mg.
ACTION Capsules, Extended-Release: (Effexor
Potentiates CNS neurotransmitter activity XR): 37.5 mg, 75 mg, 150 mg. Tablets,
by inhibiting reuptake of serotonin, nor- Extended-Release: 37.5 mg, 75 mg, 150
epinephrine, and, to lesser degree, DO- mg, 225 mg.
Pamine. Therapeutic Effect: Relieves
depression. ADMINISTRATION/HANDLING
PO
PHARMACOKINETICS • Give with food. • Scored tablet may
Well absorbed from GI tract. Protein be crushed. • Do not break, crush, dis-
binding: 25%–30%. Metabolized in liver. solve, or divide extended-release tab-
Primarily excreted in urine. Not removed lets. • May open capsule, sprinkle on
by hemodialysis. Half-life: 3–7 hrs; applesauce. Give immediately without
metabolite, 9–13 hrs (increased in he- chewing and follow with full glass of water.
patic/renal impairment).
INDICATIONS/ROUTES/DOSAGE
LIFESPAN CONSIDERATIONS Depression
Pregnancy/Lactation: Unknown if dis- PO: (Immediate-Release): ADULTS, EL-
tributed in breast milk. Children: Chil- DERLY: Initially, 37.5–75 mg/day in 2–3
dren, adolescents are at increased risk for divided doses with food. May increase up
suicidal ideation and behavior, worsening to 75 mg/day at intervals of 4 days or lon-
depression, esp. during first few mos of ger. Usual dose: 75–225 mg/day. Maxi-
therapy. Elderly: Use caution. mum: 375 mg/day in 3 divided doses.
PO: (Extended-Release): ADULTS,
INTERACTIONS ELDERLY: Initially, 37.5–75 mg/day as
DRUG: CYP3A4 inhibitors (e.g., clar­ single dose with food. May increase by V
ithromycin, ketoconazole) may in- 75 mg/day at intervals of 4 days or lon-
crease concentration/effects. MAOIs (e.g., ger. Usual dose: 75–225 mg once daily.
phenelzine, selegiline) may cause neu- Maximum: 225 mg/day.
roleptic malignant syndrome, autonomic
instability (including rapid fluctuations of Generalized Anxiety Disorder (GAD)
vital signs), extreme agitation, hyperther- PO: (Extended-Release): ADULTS, EL-
mia, altered mental status, myoclonus, DERLY: Initially, 37.5–75 mg/day (pts ini-
rigidity, coma. Strong CYP3A4 induc- tiated at 37.5 mg once daily may increase
ers (e.g., carBAMazepine, phenytoin, to 75 mg once daily after 4–7 days). May
rifAMPin) may decrease concentration/ increase by 75 mg/day at 4-day intervals
effect. May increase risk of bleeding with up to 225 mg/day.

Canadian trade name Non-Crushable Drug High Alert drug


1212 verapamil
Panic Disorder hours for drowsiness, dizziness, anxiety;
PO: (Extended-Release): ADULTS, provide assistance as necessary. Assess
ELDE­RLY: Initially, 37.5 mg/day. May appearance, behavior, speech pattern,
increase to 75 mg after 7 days followed level of interest, mood for therapeutic
by increases of 75 mg/day at 7-day in- response. Monitor for suicidal ideation
tervals up to 225 mg/day. (esp. at initiation of therapy or changes
in dosage).
Social Anxiety Disorder (SAD)
PO: (Extended-Release): ADULTS, EL- PATIENT/ FAMILY TEACHING
DERLY: 75 mg once daily. • Take with food to minimize GI dis-
tress. • Do not increase, decrease, sud-
Dosage in Renal/Hepatic Impairment denly stop medication. • Avoid tasks
Consider decreasing venlafaxine dosage that require alertness, motor skills until
by 50% in pts with moderate hepatic im- response to drug is established. • Re-
pairment, 25% in pts with mild to mod- port if breastfeeding, pregnant, or plan-
erate renal impairment, 50% in pts on ning to become pregnant. • Avoid alco-
dialysis (withhold dose until completion hol. • Report worsening depression,
of dialysis). When discontinuing therapy, suicidal ideation, unusual changes in
taper dosage slowly over 2 wks. behavior.
SIDE EFFECTS
Frequent (greater than 20%): Nausea,
drowsiness, headache, dry mouth. Oc-
casional (20%–10%): Dizziness, insom-
verapamil
nia, constipation, diaphoresis, nervous- ver-ap-a-mil
ness, asthenia, ejaculatory disturbance, (Calan, Calan SR, Verelan, Verelan
anorexia. Rare (less than 10%): Anxiety, PM, Covera-HS , Isoptin SR )
blurred vision, diarrhea, vomiting, Do not confuse Calan with
tremor, abnormal dreams, impotence. Covera-HS or Verelan with
ADVERSE EFFECTS/TOXIC Voltaren.
REACTIONS FIXED-COMBINATION(S)
Sustained increase in diastolic B/P of Tarka: verapamil/trandolapril (an ACE
10–15 mm Hg occurs occasionally. Se- inhibitor): 240 mg/1 mg, 180 mg/
rotonin syndrome (agitation, confusion, 2 mg, 240 mg/2 mg, 240 mg/4 mg.
hallucinations, hyperreflexia), neurolep-
tic malignant syndrome (muscular rigid- uCLASSIFICATION
ity, fever, cognitive changes), suicidal PHARMACOTHERAPEUTIC: Calcium
ideation have occurred. channel blocker (nondihydropyri-
V NURSING CONSIDERATIONS dine). CLINICAL: Antihypertensive,
antianginal, antiarrhythmic (class
BASELINE ASSESSMENT IV).
Obtain initial weight, B/P. Assess ap-
pearance, behavior, speech pattern,
USES
level of interest, mood. Assess risk of
suicide. Parenteral: Management of supraven-
tricular tachyarrhythmias (SVT, rapid
INTERVENTION/EVALUATION conversion to sinus rhythm), temporary
Monitor signs/symptoms of depression, control of rapid ventricular rate in atrial
B/P, weight. Assess sleep pattern for evi- flutter/fibrillation. PO: Treatment of
dence of insomnia. Check during waking angina at rest (e.g., vasospastic angina,

underlined – top prescribed drug


verapamil 1213
unstable angina, chronic stable angina). INTERACTIONS
Control of ventricular rate at rest and DRUG: May increase hypotensive effect
during stress in chronic atrial flutter of beta blockers (e.g., carvedilol,
and/or fibrillation. Management of hy- metoprolol). May increase concen-
pertension. Prophylaxis of repetitive tration/effects of statins (e.g., ator-
paroxysmal supraventricular tachycar- vastatin, simvastatin), dofetilide.
dia (PSVT). Strong CYP3A4 inhibitors (e.g.,
clarithromycin, ketoconazole) may
PRECAUTIONS
increase concentration/effect. May in-
Contraindications: Hypersensitivity to crease concentration of cycloSPORINE,
verap­amil. Atrial fibrillation/flutter in pres- carBAMazepine. CYP3A4 inducers
ence of accessory bypass tract (e.g., (e.g., carBAMazepine, phe­ nytoin,
Wolff-Parkinson-White, Lown-Ganong- rifAMPin) may ­decrease c­ oncentration/
Levine syndromes), severe left ventricu- effect. HERBAL: St. John’s wort may
lar dysfunction, cardiogenic shock, sec- decrease concentration/effect. Herb-
ond- or third-degree heart block (except als with hypertensive properties
with pacemaker), hypotension (SBP less (e.g., licorice, yohimbe) or hypo-
than 90 mm Hg), sick sinus syndrome tensive properties (e.g., garlic, gin-
(except with pacemaker). IV: Current ger, ginkgo biloba) may alter effects.
use of IV beta-blocking agents, ventricu- FOOD: Grapefruit products may in-
lar tachycardia. Cautions: Renal/hepatic crease concentration/effect. LAB VAL-
impairment, concomitant use of beta UES: ECG may show prolonged PR inter-
blockers and/or digoxin, myasthenia val. Therapeutic serum level: 0.08–0.3
gravis, elderly pts, hypertrophic cardio- mcg/mL; toxic serum level: N/A.
myopathy. Avoid use in HF.
AVAILABILITY (Rx)
ACTION
Injection Solution: 2.5 mg/mL. Tab-
Inhibits calcium ion entry across cardiac, lets: 40 mg, 80 mg, 120 mg.
vascular smooth-muscle cell membranes,
Capsules, Extended-Release: 100
dilating coronary arteries, peripheral
mg, 120 mg, 180 mg, 200 mg, 240 mg,
arteries, arterioles. Therapeutic Ef-
300 mg, 360 mg. Tablets, Extended-Re-
fect: Decreases heart rate, myocardial
lease: 120 mg, 180 mg, 240 mg.
contractility; slows SA, AV conduction.
Decreases total peripheral vascular resis- ADMINISTRATION/HANDLING
tance by vasodilation.
IV
PHARMACOKINETICS
Reconstitution • May give undiluted.
Well absorbed from GI tract. Protein bind- Rate of administration • Administer
ing: 90% (60% in neonates). Metabolized IV push over 2 min for adults, children;
in liver. Primarily excreted in urine. Not give over 3 min for elderly. • Continu- V
removed by hemodialysis. Half-life: Sin- ous ECG monitoring during IV injection
gle dose: 2–8 hrs; multiple doses: is required for children, recommended
4.5–12 hrs. for adults. • Monitor ECG for rapid
ventricular rate, extreme bradycardia,
LIFESPAN CONSIDERATIONS
heart block, asystole, prolongation of PR
Pregnancy/Lactation: Drug crosses interval. Notify physician of any signifi-
placenta; distributed in breast milk. cant changes. • Monitor B/P q5–
Breastfeeding not recommended. Chil- 10min. • Pt should remain recumbent
dren: No age-related precautions noted. for at least 1 hr after IV administration.
Elderly: Age-related renal impairment Storage • Store vials at room temper-
may require dosage adjustment. ature.
Canadian trade name Non-Crushable Drug High Alert drug
1214 verapamil
PO Hypertension
• Do not give with grapefruit products. PO: (Immediate-Release): ADULTS,
• Do not crush or cut extended-release ELD­ERLY:Initially, 40–120 mg 3 times/day.
tablets, capsules. Give extended-release tab- Range: 240 – 480 mg /day in divided doses.
lets with food. • Sustained-release cap- PO: (Extended-Release [Calan SR]):
sules may be opened and sprinkled on ADULTS, ELDERLY: Initially, 120–180 mg
applesauce, then swallowed immediately
­ once daily. May increase at wkly intervals
(do not chew). to 240 mg once daily, then 180 mg twice
daily. Maximum: 240 mg twice daily.
IV INCOMPATIBILITIES PO: (Extended-Release [Verelan]):
Albumin, amphotericin B complex (Abelcet, ADULTS, ELDERLY: Initially, 120–240 mg
AmBisome, Amphotec), nafcillin (Nafcil), once daily. May increase dose at wkly inter-
propofol (Diprivan), sodium bicarbonate. vals to 180 mg/day, then 240 mg/day, then
360 mg/day, then 480 mg/day maximum.
IV COMPATIBILITIES PO: (Extended-Release [Verelan PM]):
Amiodarone (Cordarone), calcium ADULTS, ELDERLY: Initially, 100–200 mg
chloride, calcium gluconate, dexa- once daily at bedtime. May increase dose at
methasone (Decadron), digoxin (Lan- wkly intervals to 300 mg once daily, then 400
oxin), DOBUTamine (Dobutrex), DO- mg once daily maximum.
Pamine (Intropin), furosemide (Lasix),
heparin, HYDROmorphone (Dilau- Chronic Atrial Fibrillation (Rate Control),
did), lidocaine, magnesium sulfate, SVT
metoclopramide (Reglan), milrinone PO: (Immediate-Release): ADULTS, EL-
(Primacor), morphine, multivitamins, DERLY: 240–480 mg/day in 3–4 divided
nitroglycerin, norepinephrine (Levo- doses. Usual range: 120–360 mg/day.
phed), potassium chloride, potassium
Dosage for Renal Impairment
phosphate, procainamide (Pronestyl),
propranolol (Inderal). CrCl less than 10 mL/min:Dose re-
duction (50%–75%) of normal dose
INDICATIONS/ROUTES/DOSAGE recommended.
Supraventricular Tachyarrhythmias (SVT) Dosage in Hepatic Impairment
IV: ADULTS, ELDERLY: Initially, 5–10 mg Dose reduction (20%–50%) of normal
over 2 min. May give 10 mg 15–30 min dose recommended.
after initial dose. CHILDREN 1–15 YRS: 0.1–
0.3 mg/kg over 2 min. Maximum initial SIDE EFFECTS
dose: 5 mg. May repeat in 15–30 min. Frequent (7%): Constipation. Occasional
Maximum second dose: 10 mg. (4%–2%): Dizziness, light-headedness,
Angina, Unstable Angina, Chronic Stable
headache, asthenia, nausea, peripheral
Angina
edema, hypotension. Rare (less than
V 1%): Bradycardia, dermatitis, rash.
PO: (Immediate-Release): ADULTS, EL-
DERLY: 80–60 mg 3 times daily. ADVERSE EFFECTS/TOXIC
Atrial Fibrillation (Rate Control)
REACTIONS
IV: ADULTS, ELDERLY: Initially, 0.075– Rapid ventricular rate in atrial flutter/fi-
0.15 mg/kg (usual: 5–10 mg) over 2 min. brillation, marked hypotension, extreme
May repeat with 10 mg after 15–30 min. bradycardia, HF, asystole, second- or
PO: (Immediate-Release): 240–480 third-degree AV block occur rarely.
mg/day in 3–4 divided doses.

underlined – top prescribed drug


vilazodone 1215

NURSING CONSIDERATIONS USES


Treatment of major depressive disorder.
BASELINE ASSESSMENT
Obtain baseline ECG. Record onset, type PRECAUTIONS
(sharp, dull, squeezing), radiation, location, Contraindications: Hypersensitivity to
intensity, duration of anginal pain, precipi- vilazodone. Use of MAOIs intended to
tating factors (exertion, emotional stress). treat psychiatric disorders (with or
Check B/P for hypotension, pulse for brady- within 14 days of stopping vilazodone
cardia immediately before giving medication. or MAOI), starting vilazodone in pts
INTERVENTION/EVALUATION
receiving linezolid or methylene blue.
Cautions: Seizure disorder, pts at risk
Assess pulse for quality, rate, rhythm. Moni- for suicide, hepatic impairment, el-
tor B/P. Monitor ECG for cardiac changes, derly pts.
particularly prolongation of PR interval.
Notify physician of any significant ECG ACTION
interval changes. Assist with ambulation Enhances serotonergic activity in CNS
if dizziness occurs. Assess for peripheral by selectively inhibiting reuptake of se-
edema. For those taking oral form, monitor rotonin. Therapeutic Effect: Relieves
daily pattern of bowel activity, stool consis- depression.
tency. Therapeutic serum level: 0.08–
0.3 mcg/mL; toxic serum level: N/A. PHARMACOKINETICS
PATIENT/FAMILY TEACHING Readily absorbed from GI tract. Peak
• Do not abruptly discontinue medica- concentration: 4–5 hrs. Widely distrib-
tion. • Compliance with therapy regimen is uted. Protein binding: 96%–99%. Me-
essential to control anginal pain. • Go from tabolized in liver. Half-life: 25 hrs.
lying to standing slowly. • Avoid tasks that LIFESPAN CONSIDERATIONS
require alertness, motor skills until response
to drug is established. • Limit caf- Pregnancy/Lactation: Unknown if drug
feine. • Avoid or limit alcohol. • Report crosses placenta or is excreted in breast
continued, persistent angina pain, irregular milk. Children: Safety and efficacy not
heartbeats, shortness of breath, swelling, diz- established. Elderly: No age-related pre-
ziness, constipation, nausea, hypotension. cautions noted.
• Avoid grapefruit products. INTERACTIONS
DRUG: Alcohol may increase adverse
effects. Lithium, MAOIs (e.g., phen-
vilazodone elzine, selegiline) may increase sero-
tonergic effect. Aspirin, NSAIDs (e.g.,
vil-az-oh-done ibuprofen, ketorolac, naproxen),
(Viibryd) warfarin may increase risk of bleed- V
j BLACK BOX ALERT j Increased ing. Strong CYP3A4 inhibitors (e.g.,
risk of suicidal ideation and behavior clarithromycin, ketoconazole) may
in children, adolescents, and young increase concentration. BusPIRone,
adults 18–24 yrs of age with major
depressive disorder, other psychiat- eletriptan, naratriptan, SNRIs (e.g.,
ric disorders. venlafaxine), SSRIs (e.g., sertra-
line), traMADol, tryptophan may
uCLASSIFICATION increase risk of serotonin syndrome.
PHARMACOTHERAPEUTIC: Selective HERBAL: Herbals with anticoagulant/
serotonin reuptake inhibitor. CLINI- antiplatelet properties (e.g., garlic,
CAL: Antidepressant. ginger, ginkgo biloba), glucosamine
may increase risk of bleeding. St. John’s
Canadian trade name Non-Crushable Drug High Alert drug
1216 vinBLAStine
wort may decrease concentration/effect. malignant syndrome (fever, muscular ri-
FOOD: None known. LAB VALUES: None gidity, cognitive changes).
significant.
NURSING CONSIDERATIONS
AVAILABILITY (Rx)
BASELINE ASSESSMENT
Tablets: 10 mg, 20 mg, 40 mg.
Assess behavior, appearance, emotional
ADMINISTRATION/HANDLING status, response to environment, speech
PO
pattern, thought content, risk of suicide.
• Give with food (administration with- INTERVENTION/EVALUATION
out food can result in inadequate Monitor B/P, heart rate, weight. Moni-
drug concentration, may diminish effec- tor for suicidal ideation (esp. at ini-
tiveness). tiation of therapy or changes in dos-
INDICATIONS/ROUTES/DOSAGE age). Assess for therapeutic response
(greater interest in surroundings,
Depression improved self-care, increased ability
PO: ADULTS, ELDERLY: Initially, 10 mg once to concentrate, relaxed facial expres-
daily for 7 days, followed by 20 mg once sion).
daily. May increase to 40 mg once daily after
a minimum of 7 days. Note: When discon- PATIENT/FAMILY TEACHING
tinuing treatment, reduce dose gradually. • Avoid tasks that may require alert-
From 40 mg/day: taper to 20 mg/day for 4 ness, motor skills until response to
days, then 10 mg/day for 3 days. From 20 drug is established (may cause dizzi-
mg/day: taper to 10 mg/day for 7 days. ness). • Slowly go from lying to
standing. • Take with food. • Do
Concomitant Moderate/Strong CYP3A4 not suddenly stop taking medication;
Inhibitors withdraw gradually. • Report suicidal
PO: ADULTS, ELDERLY: 20 mg/day. ideation, signs of mania/hypomania.
Concomitant Strong CYP3A4 Inducers
Avoid alcohol.
May increase dose to 80 mg/day when
used concomitantly for more than 14
days.
vinBLAStine
Dosage in Renal/Hepatic Impairment
No dose adjustment. vin-blas-teen

SIDE EFFECTS j BLACK BOX ALERT jMust


be administered by personnel
Frequent (28%–23%): Diarrhea, nausea. trained in administration/handling
Occasional (9%–3%): Dizziness, dry mouth, of chemotherapeutic agents. For IV
V insomnia, vomiting, decreased libido, use only. Fatal if given intrathe-
cally (ascending paralysis, death).
abnormal dreams, fatigue, sweating. Rare Vesicant; avoid extravasation.
(2%): Dyspepsia, flatulence, paresthesia,
Do not confuse vinBLAStine with
restlessness, arthralgia, abnormal orgasm, vinCRIStine or vinorelbine.
delayed ejaculation, increased appetite,
palpitations, tremor. uCLASSIFICATION

ADVERSE EFFECTS/TOXIC PHARMACOTHERAPEUTIC: Antimi-


REACTIONS crotubular. Vinca alkaloid. CLINI-
CAL: Antineoplastic.
Serotonin syndrome (agitation, confusion,
hallucinations, hyperreflexia), neuroleptic

underlined – top prescribed drug


vinBLAStine 1217

USES cladribine) may increase myelosuppres-


Treatment of Hodgkin’s lymphoma, non- sion. Live virus vaccines may potentiate
Hodgkin’s lymphoma, Langerhans cell virus replication, increase vaccine side
histiocytosis, advanced testicular carci- effects, decrease pt’s antibody response
noma, Kaposi’s sarcoma, Letterer-Siwe to vaccine. HERBAL: St. John’s wort
disease, breast carcinoma, resistant cho- may decrease concentration. Echina-
riocarcinoma. OFF-LABEL: Treatment of cea may decrease the therapeutic effect.
bladder, ovarian cancer; non–small-cell FOOD: None known. LAB VALUES: May
lung cancer; soft tissue sarcoma, mela- increase serum uric acid.
noma.
AVAILABILITY (Rx)
PRECAUTIONS Injection Solution: 1 mg/mL.
Contraindications: Hypersensitivity to vin-
ADMINISTRATION/HANDLING
BLAStine. Bacterial infection, significant
granulocytopenia (unless as a result of b ALERT c May be carcinogenic, muta-
condition being treated). Cautions: He- genic, teratogenic. Handle with extreme
patic impairment, severe leukopenia, neu- care during preparation and administra-
rotoxicity, recent exposure to radiation tion. Give by IV injection. Leakage from
therapy, chemotherapy, ischemic heart IV site into surrounding tissue may pro-
disease, preexisting pulmonary disease. duce extreme irritation. Avoid eye con-
tact with solution (severe eye irritation,
ACTION possible corneal ulceration may result).
Binds to tubulin, inhibiting microtubule If eye contact occurs, immediately irri-
formation; may interfere with nucleic gate eye with water.
acid, protein synthesis. Therapeutic Ef- IV
fect: Inhibits cell division by disrupting
mitotic spindle. Note: In order to prevent inadvertent
intrathecal administration, dispense as a
PHARMACOKINETICS piggyback (not a syringe).
Does not cross blood-brain barrier. Reconstitution • Using 1 mg/mL so-
Protein binding: 99%. Metabolized in lution, further dilute in 25–50 mL D5W
liver. Primarily excreted in feces. Half- or 0.9% NaCl.
life: 24.8 hrs. Rate of administration • Infuse over
5–15 min. Prolonged administration time
LIFESPAN CONSIDERATIONS and/or increased volume may increase
Pregnancy/Lactation: If possible, avoid risk of vein irritation and extravasation.
use during pregnancy, esp. during first tri- Storage • Refrigerate unopened vi-
mester. Breastfeeding not recommended. als. • Solution appears clear, color-
Aspermia has been reported in males. Chil- less. • Following dilution, solution is
dren/Elderly: No age-related precautions stable for up to 21 days if protected from V
noted. light (consult manufacturer prescribing
information). • Discard if solution is
INTERACTIONS discolored or precipitate forms.
DRUG: May decrease concentration/anti-
IV INCOMPATIBILITIES
convulsant effects of phenytoin. Strong
CYP3A4 inhibitors (e.g., clarithro- Furosemide (Lasix).
mycin, ketoconazole) may increase
level/toxicity. Strong CYP3A4 inducers IV COMPATIBILITIES
(e.g., carBAMazepine, phenytoin, ri- Allopurinol (Aloprim), CISplatin (Plati-
fAMPin) may decrease concentration/ef- nol AQ), cyclophosphamide (Cytoxan),
fect. Bone marrow depressants (e.g., DOXOrubicin (Adriamycin), etoposide
Canadian trade name Non-Crushable Drug High Alert drug
1218 vinBLAStine
(VePesid), 5-fluorouracil, gemcitabine is usually mild and transient, with recovery
(Gemzar), granisetron (Kytril), heparin, occurring in a few days. Hepatic insuffi-
leucovorin, methotrexate, ondansetron ciency may increase risk of toxicity. Acute
(Zofran), PACLitaxel (Taxol), vinorelbine shortness of breath, bronchospasm may
(Navelbine). occur, particularly when administered
concurrently with mitoMYcin.
INDICATIONS/ROUTES/DOSAGE
b ALERT c Dosage individualized
NURSING CONSIDERATIONS
based on clinical response, tolerance to BASELINE ASSESSMENT
adverse effects. When used in combina- Nausea, vomiting easily controlled by
tion therapy, consult specific protocols antiemetics. Discontinue therapy if WBC,
for optimum dosage, sequence of drug platelet counts fall abruptly (unless drug
administration. is clearly destroying tumor cells in bone
Usual Dosage
marrow). Obtain CBC wkly or before
IV: ADULTS, ELDERLY: Initially, 3.7 mg/ each dosing. Offer emotional support.
m2 (adjust dose q7days based on WBC INTERVENTION/EVALUATION
response) up to 5.5 mg/m2 (second If neutrophils fall below 2,000 cells/
wk), 7.4 mg/m2 (third wk), 9.25 mg/m2 mm3, assess diligently for signs of infec-
(fourth wk), and 11.1 mg/m2 (fifth wk). tion. Assess for stomatitis; maintain strict
Maximum: 18.5 mg/m2. CHILDREN: 3–6 oral hygiene. Monitor for hematologic
mg/m2 q7–14days. Maximum: 12.5 mg/ toxicity: infection (fever, sore throat,
m2/wk. signs of local infection), unusual bruis-
Dosage in Renal Impairment
ing/bleeding from any site, symptoms of
No dose adjustment. anemia (excessive fatigue, weakness).
Monitor daily pattern of bowel activity,
Dosage in Hepatic Impairment stool consistency. Avoid constipation. Ex-
Direct serum bilirubin concentration travasation may result in cellulitis, phle-
1.5–3 mg/dL: Reduce dose by 50%. bitis. Large amount of extravasation may
Greater than 3 mg/dL: Avoid use. result in tissue sloughing. If extravasation
occurs, give local injection of hyaluroni-
SIDE EFFECTS dase, apply warm compresses.
Frequent: Nausea, vomiting, alopecia. PATIENT/FAMILY TEACHING
Occasional: Constipation, diarrhea, rec-
tal bleeding, headache, paresthesia (oc- • Immediately report any pain/burning at
cur 4–6 hrs after administration, persist injection site during administra-
for 2–10 hrs), malaise, asthenia, dizzi- tion. • Pain at tumor site may occur
ness, pain at tumor site, jaw/face pain, during or shortly after injection. • Do
depression, dry mouth. Rare: Dermatitis, not have immunizations without physician
V approval (drug lowers resistance).
stomatitis, phototoxicity, hyperuricemia.
• Avoid crowds, those with infec-
ADVERSE EFFECTS/TOXIC tion. • Promptly report fever, sore
REACTIONS throat, signs of local infection, unusual
Hematologic toxicity manifested most bruising/bleeding from any site. • Hair
commonly as leukopenia, less frequently loss is reversible, but new hair growth may
as anemia. WBC reaches its nadir 4–10 have different color, texture. • Report
days after initial therapy, recovers within persistent nausea/vomiting. • Avoid con-
7–14 days (high dosage may require 21- stipation by increasing fluids, bulk in diet,
day recovery period). Thrombocytopenia exercise as tolerated.

underlined – top prescribed drug


vinCRIStine 1219
acid/protein synthesis. Therapeutic Ef-
vinCRIStine fect: Inhibits cell division by disrupting
mitotic spindle.
vin-cris-teen
(Marqibo, Vincasar PFS) PHARMACOKINETICS
j BLACK BOX ALERT jMust Does not cross blood-brain barrier. Pro-
be administered by personnel tein binding: 75%. Metabolized in liver.
trained in administration/handling
of chemotherapeutic agents. For IV Primarily excreted in feces by biliary sys-
use only. Fatal if given intrathe- tem. Half-life: 24 hrs. Marqibo: 45 hrs.
cally (ascending paralysis, death).
Vesicant; avoid extravasation. LIFESPAN CONSIDERATIONS
Marqibo and Vincasar are not Pregnancy/Lactation: If possible, avoid
interchangeable.
use during pregnancy, esp. first trimester.
Do not confuse vinCRIStine with May cause fetal harm. Breastfeeding not
vinBLAStine. recommended. Children: No age-related
uCLASSIFICATION precautions noted. Elderly: More suscep-
tible to neurotoxic effects.
PHARMACOTHERAPEUTIC: Antimi-
crotubular. Vinca alkaloid. CLINI- INTERACTIONS
CAL: Antineoplastic.
DRUG: May decrease concentration/
anticonvulsant effects of phenytoin.
USES Itraconazole may increase severity of
neuromuscular side effects. Strong
Vincasar: Treatment of acute lymphocytic
CYP3A4 inducers (e.g., carBAM-
leukemia (ALL), Hodgkin’s lymphoma, ad-
azepine, phenytoin, rifAMPin) may
vanced non-Hodgkin’s lymphomas, neu-
decrease concentration/effect. Strong
roblastoma, rhabdomyosarcoma, Wilms
CYP3A4 inhibitors (e.g., clarithro-
tumor. Marqibo: Relapsed Philadel-
mycin, ketoconazole) may increase
phia chromosome negative (Ph−) ALL in
concentration/effect. Live virus vaccines
adults whose disease has progressed after
may potentiate virus replication, increase
2 or more antileukemic therapies. OFF-
vaccine side effects, decrease pt’s antibody
LABEL: Vincasar: Treatment of multiple
response to vaccine. HERBAL: St. John’s
myeloma, chronic lymphocytic leukemia
wort may decrease concentration/effect.
(CLL), brain tumors, small cell lung can-
Echinacea may decrease the therapeutic
cer, ovarian germ cell tumors, Ewing’s sar-
effect. FOOD: None known. LAB VAL-
coma, gestational trophoblastic tumors,
UES: May increase serum uric acid.
retinoblastoma.
AVAILABILITY (Rx)
PRECAUTIONS
Injection Solution: 1 mg/mL. Injection
Contraindications: Hypersensitivity to Suspension: (Marqibo): 5 mg/31 mL. V
vinCRIStine. Demyelinating form of Char-
cot-Marie-Tooth syndrome. Intrathecal ADMINISTRATION/HANDLING
administration. Cautions: Hepatic im- Note: In order to prevent inadvertent
pairment, pts receiving radiation therapy intrathecal administration, dispense as a
through ports (including liver), neuro- piggyback. (not a syringe).
toxicity, preexisting neuromuscular dis-
ease, hepatobiliary dysfunction, elderly. IV

ACTION b ALERT c May be carcinogenic, muta-


genic, teratogenic. Handle with extreme
Binds to tubulin, inhibiting microtubule care during preparation and administra-
formation; may interfere with nucleic tion. Use extreme caution in calculating,

Canadian trade name Non-Crushable Drug High Alert drug


1220 vinCRIStine
administering vinCRIStine. Overdose may DREN WEIGHING LESS THAN 10 KG: 0.05 mg/
result in serious or fatal outcome. kg once wkly. Maximum: 2 mg.
Injection Solution Dosage in Renal Impairment
Reconstitution • Dilute in 25–50 mL No dose adjustment.
D5W or 0.9% NaCl.
Rate of administration • Administer Dosage in Hepatic Impairment
as 5–10 min infusion (preferred). • Do Bilirubin Dosage
not inject into extremity with impaired, Bilirubin greater 50% of normal
potentially impaired circulation caused than 3 mg/dL
by compression or invading neoplasm,
phlebitis, varicosity. ALL Injection Suspension
Storage • Refrigerate unopened vi- IV: ADULTS, ELDERLY: 2.25 mg/m2 q7days.
als. • Solution appears clear, color- Infuse over 1 hr.
less. • Discard if solution is discolored
or precipitate forms. • Diluted solu- Dosage in Renal/Hepatic Impairment
tions are stable for 7 days refrigerated or No dose adjustment.
2 days at room temperature.
Injection Suspension
SIDE EFFECTS
• Calculate dose of vinCRIStine and re- Expected: Peripheral neuropathy (oc-
move volume equal to volume of in- curs in nearly every pt; first clinical
tended solution from 100 mL 0.9% NaCl sign is depression of Achilles tendon
or D5W infusion bag. Inject vinCRIStine reflex). Frequent: Peripheral paresthe-
into infusion bag (total volume: 100 mL). sia, alopecia, constipation/obstipation
Rate of administration • Administer (upper colon impaction with empty
over 60 min. rectum), abdominal cramps, head-
Storage • Solution must be adminis- ache, jaw pain, hoarseness, diplopia,
tered within 12 hrs of preparation. ptosis/drooping of eyelid, urinary tract
disturbances. Occasional: Nausea,
IV INCOMPATIBILITIES vomiting, diarrhea, abdominal dis-
Furosemide (Lasix), IDArubicin (Idamy- tention, stomatitis, fever. Rare: Mild
cin). leukopenia, mild anemia, thrombocy-
topenia.
IV COMPATIBILITIES
Allopurinol (Aloprim), CISplatin (Plati- ADVERSE EFFECTS/TOXIC
nol AQ), cyclophosphamide (Cytoxan), REACTIONS
cytarabine (Ara-C, Cytosar), DOXOrubi- Acute dyspnea, bronchospasm may oc-
cin (Adriamycin), etoposide (VePesid), cur, esp. when administered concur-
5-fluorouracil, gemcitabine (Gemzar), rently with mitoMYcin. Prolonged or
V granisetron (Kytril), leucovorin, metho- high-dose therapy may produce foot/
trexate, ondansetron (Zofran), PACLi- wrist drop, difficulty walking, slapping
taxel (Taxol), vinorelbine (Navelbine). gait, ataxia, muscle wasting. Acute uric
acid nephropathy may occur.
INDICATIONS/ROUTES/
DOSAGE NURSING CONSIDERATIONS
Usual Dosage Injection Solution
BASELINE ASSESSMENT
IV: ADULTS, ELDERLY: 1.4 mg/m2, frequency
may vary based on protocol. CHILDREN Obtain baseline CBC, LFT. Offer emo-
WEIGHING MORE THAN 10 KG: 1.5–2 mg/m2, tional support. Question history of
frequency may vary based on protocol. CHIL-

underlined – top prescribed drug


vinorelbine 1221
hepatic impairment, neuromuscular USES
disease. Single agent or in combination with
INTERVENTION/EVALUATION CISplatin for treatment of unresectable,
advanced or metastatic, non–small-cell
Monitor serum uric acid levels, renal/
lung cancer (NSCLC). OFF-LABEL: Treat-
hepatic function studies, CBC. Assess
ment of metastatic breast cancer, cervical
Achilles tendon reflex. Monitor daily
carcinoma, ovarian carcinoma, malig-
pattern of bowel activity, stool con-
nant pleural mesothelioma, soft tissue
sistency. Monitor for ptosis, diplopia,
sarcoma, small-cell lung cancer.
blurred vision. Question pt regard-
ing urinary changes. Extravasation PRECAUTIONS
produces stinging, burning, edema at
Contraindications: Hypersensitivity to
injection site. Terminate injection im-
vinorelbine. Cautions: Compromised
mediately, locally inject hyaluronidase,
marrow reserve due to prior chemo-
apply heat (disperses drug, minimizes
therapy/radiation therapy; hepatic im-
discomfort, cellulitis).
pairment, neurotoxicity, neuropathy,
PATIENT/FAMILY TEACHING pulmonary impairment.
• Immediately report any pain/burning
at injection site during administra-
ACTION
tion. • Hair loss is reversible, but new Binds to tubulin, inhibiting microtubule
hair growth may have different color/ formation; may interfere with nucleic
texture. • Report persistent nausea/ acid protein synthesis. Therapeutic Ef-
vomiting. • Report signs of peripheral fect: Prevents cellular division by dis-
neuropathy (burning/numbness of bot- rupting formation of mitotic spindle.
tom of feet, palms of hands). • Report
fever, sore throat, unusual bleeding/
PHARMACOKINETICS
bruising, shortness of breath. Widely distributed after IV administra-
tion. Protein binding: 80%–90%. Metab-
olized in liver. Primarily excreted in feces
by biliary system. Half-life: 28–43 hrs.
LIFESPAN CONSIDERATIONS
vinorelbine Pregnancy/Lactation: If possible,
avoid use during pregnancy, esp. dur-
vin-oh-rel-been ing first trimester. May cause fetal harm.
(Navelbine) Unknown if distributed in breast milk.
j BLACK BOX ALERT j Must be Breastfeeding not recommended. Chil-
administered by personnel trained dren: Safety and efficacy not estab-
in administration/handling of lished. Elderly: No age-related precau-
chemotherapeutic agents. Severe tions noted. V
myelosuppression, resulting in
serious infections, shock, death,
may occur. INTERACTIONS
Do not confuse vinorelbine with DRUG: CISplatin may increase risk of
vinBLAStine or vinCRIStine. granulocytopenia. Live virus vaccines
may potentiate virus replication, in-
uCLASSIFICATION crease vaccine side effects, decrease pt’s
PHARMACOTHERAPEUTIC: Antimi- antibody response to vaccine. Strong
crotubular. Vinca alkaloid. CLINI- CYP3A4 inhibitors (e.g., clarithro-
CAL: Antineoplastic. mycin, ketoconazole) may increase

Canadian trade name Non-Crushable Drug High Alert drug


1222 vinorelbine
concentration/effects. HERBAL: St. John’s IV INCOMPATIBILITIES
wort may decrease concentration. Echi- Acyclovir (Zovirax), allopurinol (Al-
nacea may decrease the therapeutic effect. oprim), amphotericin B (Fungizone),
FOOD: None known. LAB VALUES: May amphotericin B complex (Abelcet, Am-
increase serum bilirubin, alkaline phos- Bisome, Amphotec), ampicillin (Om-
phatase, ALT, AST. nipen), ceFAZolin (Ancef), cefTRIAX-
AVAILABILITY (Rx) one (Rocephin), cefuroxime (Zinacef),
5-fluorouracil (5-FU), furosemide
Injection Solution: 10 mg/mL (1-mL,
(Lasix), ganciclovir (Cytovene), meth-
5-mL vials).
ylPREDNISolone (SOLU-Medrol), so-
ADMINISTRATION/HANDLING dium bicarbonate.
IV
IV COMPATIBILITIES
b ALERT c IV needle, catheter must be Calcium gluconate, CARBOplatin
correctly positioned before administration. (Paraplatin), CISplatin (Platinol AQ),
Leakage into surrounding tissue produces cyclophosphamide (Cytoxan), cytara-
extreme irritation, local tissue necrosis, bine (ARA-C, Cytosar), dacarbazine
thrombophlebitis. Handle drug with ex- (DTIC), DAUNOrubicin (Cerubidine),
treme care during administration; wear dexamethasone (Decadron), diphen-
protective clothing per protocol. If solution hydrAMINE (Benadryl), DOXOrubicin
comes in contact with skin/mucosa, imme- (Adriamycin), etoposide (VePesid),
diately wash thoroughly with soap, water. gemcitabine (Gemzar), granisetron
Reconstitution • Must be diluted and (Kytril), HYDROmorphone (Dilau-
administered via syringe or IV bag. did), IDArubicin (Idamycin), metho-
Syringe Dilution trexate, morphine, ondansetron
• Dilute calculated vinorelbine dose (Zofran), vinBLAStine (Velban), vin-
with D5W or 0.9% NaCl to concentration CRIStine (Oncovin).
of 1.5–3 mg/mL.
IV Bag Dilution INDICATIONS/ROUTES/DOSAGE
• Dilute calculated vinorelbine dose with b ALERT c Dosage adjustments should
D5W, 0.45% or 0.9% NaCl, 5% dextrose be based on granulocyte count obtained
and 0.45% NaCl, Ringer’s or lactated Ring- on the day of treatment, as follows:
er’s to concentration of 0.5–2 mg/mL.
Granulocyte Count
Rate of administration • Administer
(cells/mm3) on
diluted vinorelbine over 6–10 min into
Day of Treatment Dosage
side port of free-flowing IV closest to IV
1,500 or higher 100% of starting dose
bag followed by flushing with 75–125 mL
1,000–1,499 50% of starting dose
of one of the solutions. • If extravasa- Less than 1,000 Do not administer
tion occurs, stop injection immediately;
V give remaining portion of dose into an-
NSCLC Monotherapy
other vein.
IV injection: ADULTS, ELDERLY: 30 mg/
Storage • Refrigerate unopened vi-
m2 q7 days.
als. • Protect from light. • Unopened
vials are stable at room temperature for NSCLC Combination Therapy with
72 hrs. • Do not administer if particu- CISplatin
late has formed. • Diluted vinorelbine IV injection: ADULTS, ELDERLY: 25–30
may be used for up to 24 hrs under mg/m2 q7 days.
normal room light when stored in poly-
propylene syringes or polyvinyl chloride
bags at room temperature.

underlined – top prescribed drug


vismodegib 1223
Dosage in Renal Impairment INTERVENTION/EVALUATION
No dose adjustment. HD: Decrease dose Diligently monitor injection site for
to 20 mg/m2/wk given post-HD or on swelling, redness, pain. Frequently
non-HD days. monitor for myelosuppression during
and following therapy (infection [fever,
Dosage in Hepatic Impairment
sore throat, signs of local infection],
Serum Bilirubin Dosage unusual bleeding/bruising, anemia [ex-
2 mg/dL or less 100% of dose cessive fatigue, weakness]). Monitor pts
2.1–3 mg/dL 50% of dose developing severe granulocytopenia for
Greater than 3 mg/dL 25% of dose
evidence of infection, fever. Crackers,
dry toast, sips of cola may help relieve
SIDE EFFECTS nausea. Monitor daily pattern of bowel
Frequent (35%–12%): Asthenia, nau- activity, stool consistency. Question for
sea, constipation, erythema, pain, vein tingling, burning, numbness of hands/
discoloration at injection site, fatigue, feet (peripheral neuropathy). Pt com-
peripheral neuropathy manifested as plaint of “walking on glass” is sign of
paresthesia, hyperesthesia, diarrhea, alo- hyperesthesia.
pecia. Occasional (10%–5%): Phlebitis, PATIENT/FAMILY TEACHING
dyspnea, loss of deep tendon reflexes.
Rare: Chest pain, jaw pain, myalgia, ar-
• Immediately report redness, swell-
thralgia, rash. ing, pain at injection site. • Avoid
crowds, those with infection. • Do not
ADVERSE EFFECTS/TOXIC have immunizations without physician’s
REACTIONS approval. • Promptly report fever,
Bone marrow depression is manifested signs of infection, unusual bruising/
mainly as granulocytopenia (may be bleeding from any site, difficulty breath-
severe). Other hematologic toxicities ing. • Avoid pregnancy. • Hair loss
(neutropenia, thrombocytopenia, leuko- is reversible, but new hair growth may
penia, anemia) increase risk of infection, have different color, texture.
bleeding. Acute shortness of breath, se-
vere bronchospasm occur infrequently,
particularly in pts with preexisting pul-
monary dysfunction. Hepatic toxicity may vismodegib
occur.
vis-moe-deg-ib
NURSING CONSIDERATIONS (Erivedge)
BASELINE ASSESSMENT j BLACK BOX ALERT jMay re-
sult in embryo-fetal death or severe
Review medication history. Obtain CBC birth defects including missing
prior to each dose. Granulocyte count digits, midline defects, irreversible V
should be at least 1,000 cells/mm3 before malformations due to embryotoxic
and teratogenic properties. Verify
vinorelbine administration. Granulocyte pregnancy status prior to initiation.
nadirs occur 7–10 days following dos- Advise use of effective contracep-
ing. Do not give hematologic growth fac- tion in female pts. Advise male pts
tors within 24 hrs before administration of potential exposure risk through
of chemotherapy or earlier than 24 hrs seminal fluid.
following cytotoxic chemotherapy. Advise uCLASSIFICATION
women of childbearing potential to avoid PHARMACOTHERAPEUTIC: Hedge-
pregnancy during drug therapy. Offer hog pathway inhibitor. CLINICAL: An-
emotional support. tineoplastic.

Canadian trade name Non-Crushable Drug High Alert drug


1224 vismodegib

USES sodium, GFR. May increase serum BUN,


Treatment of adult pts with metastatic creatinine.
basal cell carcinoma, locally advanced AVAILABILITY (Rx)
basal cell carcinoma with recurrence af-
ter surgery, or pts who are not candidates Capsules: 150 mg.
for surgery or radiation.
ADMINISTRATION/HANDLING
PRECAUTIONS PO
b ALERT c Do not donate blood prod- • Give without regard to food. • Give
ucts for at least 7 mos after discontinua- whole. Do not break, crush, or open
tion. capsule.
Contraindications: Hypersensitivity to vis-
modegib. Cautions: Hepatic/renal impair- INDICATIONS/ROUTES/DOSAGE
ment. History of significant cardiac disease. Advanced or Metastatic Basal Cell
Carcinoma
ACTION PO: ADULTS/ELDERLY: 150 mg once daily.
An inhibitor of Hedgehog pathway, bind- Continue until disease progression or un-
ing to and inhibiting smoothened, a trans- acceptable toxicity.
membrane protein involved in Hedgehog
Dosage in Renal/Hepatic Impairment
signal transduction. Therapeutic Ef-
fect: Inhibits tumor cell growth and me- No dose adjustment.
tastasis of basal cell carcinoma. SIDE EFFECTS
PHARMACOKINETICS Frequent (71%–40%): Muscle spasm,
alopecia, dysgeusia, weight loss, fatigue.
Metabolized in liver. Protein binding:
Occasional (30%–11%): Nausea, amenor-
99%. Excreted in feces (82%), urine
rhea, diarrhea, anorexia, constipation,
(4%). Half-life: 4 days (daily dosing),
vomiting, arthralgia, loss of taste.
12 days (single dose).
ADVERSE EFFECTS/TOXIC
LIFESPAN CONSIDERATIONS REACTIONS
Pregnancy/Lactation: May cause fe- May cause spontaneous abortion, fetal
tal harm. Not recommended in nurs- demise, birth defects. Azotemia (renal
ing mothers. Must either discontinue impairment) reported in 2% of pts.
drug or discontinue breastfeeding.
Unknown if distributed in breast milk. NURSING CONSIDERATIONS
Contraception recommended prior
to first dose, during treatment and up BASELINE ASSESSMENT
to 24 mos after discontinuation. Dur- Obtain negative pregnancy test (urine/
ing treatment (including interruption) serum) before initiation, BMP. Ques-
V and for 3 mos after treatment, male pts tion current breastfeeding status. Assess
should not donate sperm and should skin, moles for other possible malignan-
use condoms with spermicide if part- cies. Offer emotional support.
ner is of childbearing potential. Chil- INTERVENTION/EVALUATION
dren: Safety and efficacy not estab-
lished. Elderly: Safety and efficacy not Obtain STAT human chorionic gonado-
established. tropin (HCG) level if pregnancy sus-
pected, BMP if electrolyte imbalance or
INTERACTIONS renal impairment suspected. Encourage
DRUG: None significant. HERBAL: fluid intake if diarrhea occurs. Offer
None significant. FOOD: None known. antiemetics for nausea/vomiting. Report
LAB VALUES: May decrease potassium,
oliguria, dark or concentrated urine.

underlined – top prescribed drug


vitamin D 1225
PATIENT/FAMILY TEACHING USES
• Avoid pregnancy. • May cause birth Calcitriol: Manage hypocalcemia in
defects or miscarriage. • Do not pts on chronic renal dialysis, secondary
breastfeed. • Male pts must use con- hypoparathyroidism in chronic kidney
doms with spermicide during sexual ac- disease (CKD), manage hypocalcemia
tivity, despite history of vasectomy. • Fe- in hypoparathyroidism. (Topical):
male pts must use contraception for at Treatment of mild to moderate plaque
least 7 mos after stopping treat- psoriasis. Doxercalciferol: Treatment
ment. • Immediately report suspected of secondary hyperparathyroidism in
pregnancy. • Do not donate blood for CKD. Ergocalciferol: Treatment of re-
at least 7 mos after stopping treat- fractory rickets, hypophosphatemia, hy-
ment. • Swallow capsules whole; do poparathyroidism, dietary ­supplement.
not break, crush, or open. • Hair loss ­Paricalcitol: (Intravenous): Treat-
is an expected side effect. • Strictly ment/prevention of secondary hyper-
monitor menstrual cycle. • Report parathyroidism associated with stage
dark-colored urine or decreased urine 5 CKD. (PO): Treatment/prevention of
output despite hydration. secondary hyperparathyroidism associ-
ated with stage 3 and 4 CKD and stage 5
CKD pts on hemodialysis or peritoneal
dialysis. OFF-LABEL: Calcitriol: Vitamin
vitamin D (vitamin D D–dependent rickets. Ergocalciferol:
analogues) Prevention/treatment of vitamin D de-
ficiency in pts with CKD, osteoporosis
prevention.
calcitriol
PRECAUTIONS
kal-si-trye-ole Contraindications: Hypersensitivity to
(Calcijex , Rocaltrol, Vectical) cholecalciferol, ergocalciferol. Vitamin
D toxicity, hypercalcemia. Cautions: Pts
doxercalciferol with malabsorption syndrome. Concur-
rent use with digoxin.
dox-er-kal-sif-e-role
(Hectorol) ACTION
Calcitriol: Stimulates calcium trans-
port in intestines, resorption in bones,
ergocalciferol and tubular reabsorption in kidney;
suppresses parathyroid hormone
er-goe-kal-sif-e-role (PTH) secretion/synthesis. Doxer-
(Drisdol) calciferol: Regulates blood calcium V
levels, stimulates bone growth, sup-
paricalcitol presses PTH secretion/synthesis.
Ergocalciferol: Promotes active ab-
par-i-kal-si-tol sorption of calcium and phosphorus,
(Zemplar) increasing serum levels to allow bone
mineralization; mobilizes calcium
uCLASSIFICATION and phosphate from bone, increases
PHARMACOTHERAPEUTIC: Fat-sol- reabsorption of calcium and phos-
uble vitamin. CLINICAL: Vitamin D phate by renal tubules. Paricalcitol:
analogue. Suppresses PTH secretion/synthesis.

Canadian trade name Non-Crushable Drug High Alert drug


1226 vitamin D
Therapeutic Effect: Essential for Ergocalciferol
absorption, utilization of calcium, Capsules: (Drisdol): 50,000 units (1.25
phosphate, control of PTH levels. mg). Liquid, Oral: (Drisdol): 8,000 units/
mL (200 mcg/mL). Tablets: 400 units.
PHARMACOKINETICS Paricalcitol
Calcitriol: Rapidly absorbed. Protein Capsules, Gelatin: (Zemplar): 1 mcg, 2
binding: 99.9%. Metabolized to active mcg, 4 mcg. Injection Solution: (Zem-
metabolite (ergocalciferol). Excreted plar): 2 mcg/mL.
in feces (49%), urine (16%). Half-
life: 5–8 hrs. Doxercalciferol: Me- ADMINISTRATION/HANDLING
tabolized in liver. Half-life: 32–37 Calcitriol
hrs. Ergocalciferol: Metabolized in
PO
liver. Paricalcitol: Readily absorbed.
Protein binding: 99.8%. Metabolized in • May take without regard to food.
liver. Primarily excreted in feces. Half- IV
life: 5–7 hrs.
• May give as IV bolus at end of dialysis.
LIFESPAN CONSIDERATIONS
Doxercalciferol
Pregnancy/Lactation: Unknown if
drug crosses placenta. Infant risk can- PO
not be excluded. Children/Elderly: No • May take without regard to food.
age-related precautions noted. IV

• May give as IV bolus via catheter at


INTERACTIONS end of dialysis.
DRUG: Calcium-containing prod-
ucts, concurrent vitamin D (or Ergocalciferol
derivatives) may increase risk of hy- PO
percalcemia. May increase digoxin tox- • May take without regard to food.
icity due to hypercalcemia (may cause
arrhythmias). May increase concentra- Paricalcitol
tion/effect of aluminum hydroxide, PO
sucralfate. Bile acid sequestrants • May take without regard to
(e.g., cholestyramine) may decrease food. • For 3 times/wk dosing, give no
absorption. HERBAL: None significant. more frequently than every other day.
FOOD: None known. LAB VALUES: May IV
increase serum cholesterol, calcium,
magnesium, phosphate, ALT, AST, BUN, • Give bolus anytime during dialy-
creatinine. sis. • Do not give more frequently than
V every other day.
AVAILABILITY (Rx) INDICATIONS/ROUTES/DOSAGE
Calcitriol
Calcitriol
Capsules, Softgel: (Rocaltrol): 0.25 mcg,
0.5 mcg. Injection Solution: 1 mcg/mL. Hypocalcemia on Chronic Renal Dialysis
Oral Solution: (Rocaltrol): 1 mcg/mL. PO: ADULTS, ELDERLY: (Rocaltrol): Ini-
tially, 0.25 mcg/day or every other day.
Doxercalciferol May increase by 0.25 mcg/day at 4- to
Capsules, Softgel: (Hectorol): 0.5 mcg, 1 8-wk intervals. Range: 0.5–1 mcg/day.
mcg, 2.5 mcg. Injection Solution: (Hec- IV: ADULTS, ELDERLY: 1–2 mcg 3 times/
torol): 2 mcg/mL. wk. Adjust dose at 2- to 4-wk intervals.
Range: 0.5–4 mcg 3 times/wk.
underlined – top prescribed drug
vitamin D 1227
Hypocalcemia in Hypoparathyroidism Plaque Psoriasis
PO: ADULTS, CHILDREN 6 YRS AND OLDER: Topical: ADULTS, ELDERLY: Apply to af-
(Rocaltrol): Initially, 0.25 mcg/day. May in- fected area twice daily.
crease at 2- to 4-wk intervals. Range: 0.5–2
mcg/day. CHILDREN 1–5 YRS: 0.25–0.75 mcg Paricalcitol
once daily. Secondary Hyperparathyroidism in Stage
5 CKD
Secondary Hyperparathyroidism IV: ADULTS, ELDERLY, CHILDREN 5 YRS AND
Associated with Moderate to Severe CKD OLDER: Initially, 0.04–0.1 mcg/kg given
Not on Dialysis as bolus dose no more frequently than
PO: ADULTS, ELDERLY, CHILDREN 3 YRS every other day at any time during dialy-
AND OLDER: (Rocaltrol): Initially, 0.25 sis. May increase by 2–4 mcg every 2–4
mcg/day. May increase to 0.5 mcg/day. wks. Dose is based on serum iPTH levels.
CHILDREN YOUNGER THAN 3 YRS: Initially, Secondary Hyperparathyroidism in Stages
0.01–0.015 mcg/kg/day. 3 and 4 CKD
Note: Initial dose based on baseline
Doxercalciferol serum iPTH levels. Dose adjusted q2wks
Secondary Hyperparathyroidism (Dialysis) based on iPTH levels relative to baseline.
PO: ADULTS, ELDERLY: Initial dose (in- PO: ADULTS, ELDERLY: (iPTH 500 PG/ML OR
tact parathyroid hormone [iPTH] greater LESS): 1 mcg/day or 2 mcg 3 times/wk.
than 400 pg/mL): 10 mcg 3 times/wk (iPTH GREATER THAN 500 PG/ML): 2 mcg/
at dialysis. Dose titrated to lower iPTH day or 4 mcg 3 times/wk.
to 150–300 pg/mL, with dosage adjust-
ments made at 8-wk intervals. Maxi- Dosage in Renal/Hepatic Impairment
mum: 20 mcg 3 times/wk. No dose adjustment.
IV: ADULTS, ELDERLY: Initial dose (iPTH
greater than 400 pg/mL): 4 mcg 3 times/ SIDE EFFECTS
wk after dialysis, given as bolus dose. Frequencies not defined. Calcitriol: Car-
Dose titrated to lower iPTH to 150–300 diac arrhythmias, headache, pruritus, hy-
pg/mL, with dosage adjustments made at percalcemia, polydipsia, abdominal pain,
8-wk intervals. Maximum: 18 mcg/wk. metallic taste, nausea, vomiting, myalgia,
Secondary Hyperparathyroidism soft tissue calcification. Doxercalcif-
(Predialysis) erol: Edema, pruritus, nausea, vomiting,
PO: ADULTS, ELDERLY: Initially, 1 mcg/ headache, dizziness, dyspnea, malaise,
day. Titrate dose to lower iPTH to 35–70 hypercalcemia. Ergocalciferol: Hyper-
pg/mL for stage 3 CKD and 70–110 pg/mL calcemia, hypervitaminosis D, decreased
for stage 4 CKD. Maximum: 3.5 mcg/day. renal function, soft tissue calcification,
bone demineralization, nausea, constipa-
Ergocalciferol (Dietary Supplement) tion, weight loss. Paricalcitol: Edema,
PO: ADULTS, ELDERLY, CHILDREN: 10 mcg nausea, vomiting, hypercalcemia.
(400 units)/day. NEONATES: 10–20 mcg V
(400–800 units)/day. ADVERSE EFFECTS/TOXIC
REACTIONS
Hypoparathyroidism Early signs of overdose manifested as
PO: ADULTS, ELDERLY: 625 mcg–5 mg weakness, headache, drowsiness, nau-
(25,000–200,000 units)/day (with calcium sea, vomiting, dry mouth, constipation,
supplements). CHILDREN: 1.25–5 mg muscle/bone pain, metallic taste. Later
(50,000–200,000 units)/day (with cal- signs of overdose evidenced by poly-
cium supplements). uria, polydipsia, anorexia, weight loss,
nocturia, photophobia, rhinorrhea,

Canadian trade name Non-Crushable Drug High Alert drug


1228 vorapaxar
pruritus, disorientation, hallucinations, or with active pathologic bleeding.
hyperthermia, hypertension, cardiac Antiplatelet agents increase risk of
dysrhythmias. bleeding, including ICH and fatal
bleeding.
NURSING CONSIDERATIONS uCLASSIFICATION
BASELINE ASSESSMENT PHARMACOTHERAPEUTIC: Pro-
Obtain baseline serum calcium, ionized tease-activated receptor-1 (PAR-1)
calcium, phosphorus, alkaline phospha- antagonist. CLINICAL: Antiplatelet.
tase, creatinine, PTH.

INTERVENTION/EVALUATION USES
Monitor serum, urinary calcium levels, To reduce thrombotic cardiovascular
serum phosphate, magnesium, BUN, events in pts with history of MI or periph-
creatine, alkaline phosphatase deter- eral artery disease (PAD). Reduces rate
minations (therapeutic calcium level: of a combined endpoint of cardiovascu-
9–10 mg/dL), PTH measurements. lar death, CVA, MI, and urgent coronary
Estimate daily dietary calcium intake. revascularization.
Encourage adequate fluid intake. Moni-
tor for signs/symptoms of vitamin D in- PRECAUTIONS
toxication. Contraindications: Hypersensitivity to
vorapaxar. History of stroke, intracranial
PATIENT/FAMILY TEACHING hemorrhage, transient ischemic attack;
• Adequate calcium intake should be active bleeding. Cautions: Hepatic im-
maintained. • Dietary phosphorus pairment, pts at increased risk of bleed-
may need to be restricted (foods high ing (anticoagulant use, elderly, low body
in phosphorus include beans, dairy weight, trauma) or with history of bleed-
products, nuts, peas, whole-grain ing disorders.
products). • Oral formulations may
cause hypersensitivity reactions. Avoid ACTION
excessive doses. • Report signs/ Inhibits thrombin-induced and thrombin
symptoms of hypercalcemia (head- receptor agonist peptide (TRAP)–in-
ache, weakness, drowsiness, nausea, duced platelet aggregation. Therapeutic
vomiting, dry mouth, constipation, Effect: Inhibits platelet aggregation, re-
metallic taste, muscle or bone duces incidence of thrombus.
pain). • Maintain adequate hydra-
tion. • Avoid changes in diet or sup- PHARMACOKINETICS
plemental calcium intake (unless Readily absorbed. Widely distributed.
directed by health care professional). Metabolized in liver. Protein binding:
V • Avoid magnesium-containing antac- greater than 99%. Peak plasma concen-
ids in pts with renal failure. tration: 1 hr. Steady state reached in 21
days. Excreted in feces (58%), urine
(25%). Half-life: 5–13 days.

vorapaxar LIFESPAN CONSIDERATIONS


Pregnancy/Lactation: Unknown if dis-
vor-a-pax-ar tributed in breast milk. Children: Safety
(Zontivity) and efficacy not established. Elderly: May
have increased risk of bleeding.
j BLACK BOX ALERT j Avoid
use in pts with history of CVA,
intracranial hemorrhage (ICH), TIA,

underlined – top prescribed drug


vorapaxar 1229

INTERACTIONS ADVERSE EFFECTS/TOXIC


DRUG: Aspirin, anticoagulants (e.g., REACTIONS
warfarin), NSAIDs (e.g., ibuprofen, Hemorrhagic events (25% of pts) in-
ketorolac, naproxen), serotonin cluding fatal bleeding (less than 1%),
norepinephrine reuptake inhibi- GI bleeding (4%), ICH (less than
tors (e.g., DULoxetine), SSRIs (e.g., 1%) have been reported. Vorapaxar
PARoxetine) may increase risk of increases risk of moderate to severe
bleeding. Strong CYP3A4 inducers bleeding by 55%.
(e.g., carBAMazepine, phenytoin,
rifAMPin) may decrease concentra- NURSING CONSIDERATIONS
tion/effect. Strong CYP3A4 inhibi- BASELINE ASSESSMENT
tors may increase concentration/effect.
HERBAL: St. John’s wort may decrease
Obtain baseline CBC, PFA level. Ques-
concentration/effect. Herbals with tion history of CVA, intracranial hem-
anticoagulant/antiplatelet proper- orrhage (ICH), transient ischemic at-
ties (e.g., garlic, ginger, ginkgo tack (TIA) (therapy contraindicated);
biloba), glucosamine may increase anemia, bleeding ulcers, GI/genito-
risk of bleeding. FOOD: None known. urinary (GU) bleeding, recent sur-
LAB VALUES: May decrease Hbg, Hct;
gery, spinal punctures, open wounds;
serum iron. hepatic impairment. Receive full
medication history including herbal
AVAILABILITY (Rx) products.
Tablets: 2.08 mg. INTERVENTION/EVALUATION

ADMINISTRATION/HANDLING Monitor CBC. Question for increased


menstrual bleeding/discharge. Monitor
PO for confusion, headache, hemiparesis,
• Give without regard to food. vision change (may indicate ICH); he-
INDICATIONS/ROUTES/DOSAGE maturia, GI bleeding. Assess peripheral
pulses; skin for ecchymosis, petechiae.
Reduction of Thrombotic Cardiovascular Check for excessive bleeding from mi-
Events (Pts with PAD, MI) nor cuts, scratches, skin tears. Consider
PO: ADULTS, ELDERLY: 2.08 mg once transfusion of platelets or RBCs if severe
daily (in combination with aspirin and/ bleeding occurs.
or clopidogrel).
PATIENT/FAMILY TEACHING
Dosage in Renal Impairment • It may take longer to stop bleed-
No dose adjustment. ing. • Bruising may occur more eas-
Dosage in Hepatic Impairment
ily. • Report unexpected, prolonged,
Mild to moderate impairment: No
excessive bleeding of any kind, or blood
in sputum, stool, urine, or vomi- V
dose adjustment. Severe impair-
ment: Not recommended.
tus. • Avoid alcohol, over-the-counter
anti-inflammatories such as aspirin, ibu-
SIDE EFFECTS profen, or naproxen. • Consult doctor
Rare (2%): Depression, rash, skin erup- before any planned surgery, dental
tions, exanthemas. work. • Use electric razor, soft tooth-
brush to prevent bleeding. • Report
confusion, headache, one-sided weak-
ness, trouble speaking, or vision
problems; may indicate life-threatening
bleeding of brain.

Canadian trade name Non-Crushable Drug High Alert drug


1230 voriconazole

ACTION
voriconazole Interferes with fungal cytochrome activ-
ity, decreasing ergosterol synthesis, in-
vor-i-kon-a-zole
hibiting fungal cell membrane formation.
(Vfend, Apo-Voriconazole )
Therapeutic Effect: Damages fungal
Do not confuse voriconazole cell wall membrane.
with fluconazole.
uCLASSIFICATION
PHARMACOKINETICS
Rapidly, completely absorbed after PO
PHARMACOTHERAPEUTIC: Azole de-
administration. Widely distributed. Pro-
rivative. CLINICAL: Antifungal.
tein binding: 58%. Metabolized in liver.
Primarily excreted as metabolite in urine.
USES Half-life: Variable, dose dependent.
Treatment of invasive aspergillosis, LIFESPAN CONSIDERATIONS
esophageal candidiasis. Treatment of
serious fungal infections caused by Sce- Pregnancy/Lactation: May cause fetal
dosporium apiospermum, Fusarium harm. Children: Safety and efficacy not
spp. Treatment of candidemia in non- established in pts younger than 12 yrs. El-
derly: No age-related precautions noted.
neutropenic pts. Treatment of dissemi-
nated Candida infections of skin and INTERACTIONS
abdomen, kidney, bladder wall, and
wounds. OFF-LABEL: Empiric treatment DRUG: May increase concentration, risk
of fungal meningitis or osteoarticular of toxicity of calcium channel blockers
infections, coccidioidomycosis in HIV (e.g., dilTIAZem, verapamil), cyclo-
pts, fungal endophthalmitis, infection SPORINE, ergot alkaloids, HMG-CoA
prophylaxis of graft-vs-host disease or reductase inhibitors (e.g., lovastatin),
pts with allogeneic hematopoietic stem methadone, sirolimus, tacrolimus,
cell transplant. warfarin. CarBAMazepine, rifabutin,
rifAMPin may decrease concentration/
PRECAUTIONS effect. QT interval–prolonging medi-
Contraindications: Hypersensitivity to cations (e.g., amiodarone, azithro-
voriconazole. Concurrent administra- mycin, haloperidol, moxifloxacin)
tion of barbiturates (long acting), car- may increase risk of QT interval prolon-
BAMazepine, efavirenz (400 mg/day gation, cardiac arrhythmias. HERBAL: St.
or greater), ergot alkaloids, pimozide, John’s wort may significantly decrease
quiNIDine (may cause prolonged QT concentration. FOOD: None known. LAB
VALUES: May increase serum alkaline
interval, torsades de pointes), rifabu-
tin, rifAMPin, ritonavir (800 mg/day or phosphatase, ALT, AST, bilirubin, creati-
greater), sirolimus, St. John’s wort. Cau- nine. May decrease potassium.
V
tions: Severe renal/hepatic impairment, AVAILABILITY (Rx)
hypersensitivity to other azole antifungal
agents. Pts at risk for acute pancreatitis, Injection, Powder for Reconstitution: 200
pts with fructose intolerance, glucose- mg. Powder for Oral Suspension: 200
galactose malabsorption; concomitant mg/5 mL. Tablets: 50 mg, 200 mg.
nephrotoxic medications; hypokalemia, ADMINISTRATION/HANDLING
hypomagnesemia, hypocalcemia. May
prolong QT interval; use caution in pts IV
with history of QT syndrome, concomi- Reconstitution • Reconstitute 200-mg
tant medications that prolong QT interval, vial with 19 mL Sterile Water for Injection
electrolyte imbalance.

underlined – top prescribed drug


voriconazole 1231
to provide concentration of 10 mg/mL. Candidemia, Other Deep Tissue Candida
Further dilute with 0.9% NaCl or D5W to Infections
provide concentration of 0.5–5 mg/mL. IV: ADULTS, ELDERLY, ADOLESCENTS 15 YRS
Rate of administration • Infuse over AND OLDER: Initially, 400 mg (6 mg/kg) q12h
1–2 hrs at a rate not to exceed 3 mg/kg/ for 2 doses, then 200 mg (3 mg/kg) IV or
hr. • Do not infuse concomitantly into PO q12h. CHILDREN 12–14 YRS WEIGHING 50
same line with other drug infu- KG OR MORE: 400 mg (6 mg/kg) q12h for
sions. • Do not infuse concomitantly 2 doses, then 4 mg/kg q12h. WEIGHING LESS
even in separate lines with concentrated THAN 50 KG: 9 mg/kg q12h for 2 doses,
electrolyte solutions or blood products. then 8 mg/kg q12h. CHILDREN 2–11 YRS: 9
Storage • Store powder for injection mg/kg q12h for 2 doses, then 8 mg/kg q12h.
at room temperature. • Use reconsti- PO: ADULTS, ELDERLY, ADOLESCENTS 15
tuted solution immediately. • Do not YRS AND OLDER: See IV. CHILDREN 12–14
use after 24 hrs when refrigerated. YRS WEIGHING 50 KG OR MORE: 200 mg
(3 mg/kg) q12h. WEIGHING LESS THAN 50
PO KG: 9 mg/kg q12h. Maximum: 350 mg/
• Give 1 hr before or 1 hr after a meal. dose. CHILDREN 2–11 YRS: 9 mg/kg q12h.
• Do not mix oral suspension with any Maximum: 350 mg/dose.
other medication or flavoring agent.
• Shake suspension for about 10 sec Esophageal Candidiasis
before use. PO: ADULTS, ELDERLY, ADOLESCENTS 15
YRS AND OLDER WEIGHING 40 KG OR MORE:
IV INCOMPATIBILITIES 200 mg q12h. Maximum: 600 mg daily.
Tigecycline (Tygacil). WEIGHING LESS THAN 40 KG: 100 mg q12h.
Maximum: 300 mg daily. CHILDREN 12–14
IV COMPATIBILITIES YRS WEIGHING 50 KG OR GREATER: 200
Anidulafungin, caspofungin, ceftaroline, mg q12h. WEIGHING LESS THAN 50 KG: 9
doripenem. mg/kg q12h. Maximum: 350 mg/
dose. CHILDREN 2–11 YRS: 9 mg/kg q12h.
INDICATIONS/ROUTES/DOSAGE Maximum: 350 mg/dose.
Invasive Aspergillosis
IV: ADULTS, ELDERLY, ADOLESCENTS 15 Scedosporiosis, Fusariosis
YRS AND OLDER: Initially, 6 mg/kg q12h IV: ADULTS, EDLERLY: Initially,
6 mg/kg
for 2 doses, then 4 mg/kg q12h. CHILDREN q12h for 2 doses, then 4 mg/kg q12h for
12–14 YRS WEIGHING 50 KG OR MORE: 6 mg/ at least 7 days. PO: WEIGHING 40 KG OR
kg q12h for 2 doses, then 4 mg/kg q12h. MORE: 200 mg q12h. WEIGHING LESS THAN
WEIGHING LESS THAN 50 KG: 9 mg/kg q12h 40 KG: 100 mg q12h.
for 2 doses, then 8 mg/kg q12h. CHILDREN Dosage in Pts Receiving Phenytoin
2–11 YRS: 9 mg/kg q12h for 2 doses, then
IV: Increase maintenance dose to5 mg/
8 mg/kg q12h. kg q12h. V
PO: ADULTS, ELDERLY, ADOLESCENTS
PO: Increase 200 mg q12h to 400 mg
15 YRS AND OLDER: 200–300 mg q12h q12h (pts weighing 40 kg or more) or
or 3–4 mg/kg q12h. CHILDREN 12–14 100 mg q12h to 200 mg q12h (pts weigh-
YRS WEIGHING 50 KG OR MORE: 200–
ing less than 40 kg).
300 mg q12h. WEIGHING LESS THAN
50 KG: 9 mg/kg q12h. Maximum: 350 Dosage in Pts Receiving Efavirenz
mg/dose. CHILDREN 2–11 YRS: 9 mg/kg Increase dose to 400 mg q12h and re-
q12h. Maximum: 350 mg/dose. duce efavirenz to 300 mg/day.

Canadian trade name Non-Crushable Drug High Alert drug


1232 vorinostat
Dosage in Renal Impairment
No dose adjustment. IV dosing not recom- vorinostat
mended in pts with CrCl 50 mL/min or less.
vor-in-o-stat
Dosage in Hepatic Impairment (Zolinza)
Mild to moderate impairment: Re- Do not confuse vorinostat with
duce maintenance dose by 50%. Severe Votrient.
impairment: Use only if benefits out-
weigh risks. Monitor closely for toxicity. uCLASSIFICATION
PHARMACOTHERAPEUTIC: Histone
SIDE EFFECTS deacetylase (HDAC) inhibitor. CLINI-
Frequent (20%–6%): Abnormal vision, fe- CAL: Antineoplastic.
ver, nausea, rash, vomiting. Occasional
(5%–2%): Headache, chills, hallucinations,
photophobia, tachycardia, hypertension. USES
Treatment of cutaneous manifestations
ADVERSE EFFECTS/TOXIC in pts with cutaneous T-cell lymphoma
REACTIONS (CTCL) with progressive, persistent, or
Hepatotoxicity (jaundice, hepatitis, he- recurrent disease, on or following two
patic failure), acute renal failure have systemic therapies.
occurred in severely ill pts.
PRECAUTIONS
NURSING CONSIDERATIONS Contraindications: Hypersensitivity to
BASELINE ASSESSMENT
vorinostat. Cautions: History of deep vein
thrombosis (DVT), diabetes mellitus, he-
Obtain baseline serum hepatic/renal patic impairment, preexisting hypokalemia,
function tests; ECG. Correct electrolyte hypomagnesemia, pts with history of QT
deficiencies prior to initiating treat- prolongation or medications that prolong
ment. Receive full medication history and QT interval. Use caution during periopera-
screen for interactions. Question medical tive period in pts requiring bowel surgery.
history as listed in Precautions.
ACTION
INTERVENTION/EVALUATION
Inhibits activity of histone deacetylase en-
Monitor serum renal function, LFT. Moni-
zymes that catalyze removal of acetyl groups
tor visual function (visual acuity, visual
of proteins, causing accumulation of acety-
field, color perception) for drug therapy
lated histones. Therapeutic Effect: Ter-
lasting longer than 28 days.
minates cell growth, causes apoptosis.
PATIENT/FAMILY TEACHING
PHARMACOKINETICS
• Take at least 1 hr before or 1 hr after a
meal. • Avoid grapefruit products. Protein binding: 71%. Metabolized to
V inactive metabolites. Excreted in urine.
• Avoid driving at night. • Report visual
changes (blurred vision, photophobia, Half-life: 2 hrs.
yellowing of skin/eyes). • Avoid per- LIFESPAN CONSIDERATIONS
forming hazardous tasks if changes in
vision occur. • Avoid direct sunlight. Pregnancy/Lactation: May cause fetal
• Women of childbearing potential harm. Unknown if distributed in breast
should use effective contraception. milk. Children: Safety and efficacy not
established. Elderly: No age-related pre­
cautions noted.

underlined – top prescribed drug


vortioxetine 1233

INTERACTIONS chills, vomiting, constipation, dizziness,


DRUG: May increase effect of warfa- peripheral edema, headache, pruritus,
rin. Valproic acid increases risk of cough, fever.
GI bleeding, thrombocytopenia. QT
ADVERSE EFFECTS/TOXIC
interval–prolonging medications
REACTIONS
(e.g., amiodarone, azithromycin,
haloperidol, moxifloxacin) may in- Thrombocytopenia occurs in 25% of pts,
crease risk of QT interval prolongation, anemia in 15%. Pulmonary embolism oc-
cardiac arrhythmias. HERBAL: None curs in 4% of pts. Deep vein thrombosis
significant. FOOD: None known. LAB (DVT) occurs rarely.
VALUES: May decrease serum calcium,
NURSING CONSIDERATIONS
potassium, sodium, phosphate, platelet
count. May increase serum glucose, BASELINE ASSESSMENT
creatinine; urine protein. Obtain baseline ECG. Baseline PT, INR,
CBC, serum chemistry tests, esp. serum
AVAILABILITY (Rx) potassium, calcium, magnesium, glu-
Capsules: 100 mg. cose, creatinine should be obtained prior
to therapy and every 2 wks during first
ADMINISTRATION/HANDLING 2 mos of therapy and monthly thereafter.
PO Inform women of childbearing potential
• Do not break, crush, dissolve, or di- of risk to fetus if pregnancy occurs.
vide capsules. • Give with food.
INTERVENTION/EVALUATION
• Maintain adequate hydration during
treatment. Monitor CBC, serum electrolytes; PT/INR
q2wks for 2 mos, then monthly. Monitor
INDICATIONS/ROUTES/DOSAGE signs/symptoms of DVT. Encourage fluid
Cutaneous T-Cell Lymphoma (CTCL) intake, approximately 2 L/day input. As-
PO: ADULTS, ELDERLY: 400 mg once sess for evidence of dehydration. Provide
daily with food. Continue until disease antiemetics to control nausea/vomiting.
progression or unacceptable toxicity. Monitor daily pattern of bowel activity,
stool consistency.
Dose Modification
PATIENT/FAMILY TEACHING
Intolerance or toxicity: Reduce dose
to 300 mg once daily. Unable to toler- • Drink at least 2 L/day of fluids to pre-
ate daily dose: May further reduce to vent dehydration. • Report persistent
300 mg once daily for 5 consecutive days vomiting, diarrhea. • Report shortness
per wk (5 out of 7 days). of breath, pain in any extremity.

Dosage in Renal Impairment


Use caution. vortioxetine V

Dosage in Hepatic Impairment


vor-tye-ox-e-teen
Mild to moderate impairment: 300
(Trintellix)
mg once daily. Severe impair-
ment: 100–200 mg once daily. j BLACK BOX ALERT jAntide-
pressants have an increased risk
SIDE EFFECTS of suicidal ideation and behavior
in children, adolescents, and
Frequent (50%–24%): Fatigue, diarrhea, young adults. Monitor closely for
nausea, altered taste, anorexia. Oc- worsening or emergence of suicidal
casional (21%–11%): Weight decrease, thoughts and behaviors.
muscle spasms, alopecia, dry mouth, Do not confuse vortioxetine

Canadian trade name Non-Crushable Drug High Alert drug


1234 vortioxetine

with FLUoxetine, PARoxetine, seizures, serotonin syndrome. Chil-


or venlafaxine. dren: Safety and efficacy not established
in pediatric population. Elderly: May
uCLASSIFICATION
have increased risk of dehydration, hy-
PHARMACOTHERAPEUTIC: Selective ponatremia.
serotonin reuptake inhibitor (SSRI).
CLINICAL: Antidepressant. INTERACTIONS
DRUG: Strong CYP inducers (e.g.,
carBAMazepine, phenytoin, ri-
USES
fAMPin) may decrease concentration/ef-
Treatment of major depressive disorder. fects. Strong CYP2D6 inhibitors (e.g.,
buPROPion, FLUoxetine, PARox-
PRECAUTIONS
etine) may increase concentration/effect.
Contraindications: Hypersensitivity to MAOIs (e.g., phenelzine, selegiline)
vortioxetine. Use of monoamine oxidase contraindicated; may cause malignant
inhibitors (MAOIs) intended to treat psy- hyperthermia, hypertensive crisis, hyper-
chiatric disorders concurrently or within reflexia, seizures, serotonin syndrome.
21 days of stopping vortioxetine; do not Alcohol may increase adverse effects.
use vortioxetine within 14 days of stop- Serotonergic drugs (e.g., busPIRone,
ping an MAOI. Initiation of vortioxetine linezolid, lithium, traMADol) may in-
in pts receiving linezolid or intravenous crease risk of serotonin syndrome. Anti-
methylene blue. Cautions: History of an- coagulants, antiplatelets, NSAIDs may
gioedema, dehydration, hyponatremia, increase risk of bleeding. HERBAL: St.
pts at risk for bleeding, hepatic impair- John’s wort may decrease concentration/
ment, seizure disorder, elderly pts, pts effect. Herbals with anticoagulant/an-
at high risk of suicide, family history of tiplatelet properties (e.g., garlic, gin-
bipolar disorder, mania, hypomania. ger, ginkgo biloba), glucosamine may
increase risk of bleeding. FOOD: None
ACTION
known. LAB VALUES: May decrease serum
Blocks reuptake of neurotransmitter ser- sodium.
otonin at CNS presynaptic membranes,
increasing availability at postsynaptic AVAILABILITY (Rx)
receptor sites. Therapeutic Effect: Re- Tablets: 5 mg, 10 mg, 20 mg.
lieves depression.
ADMINISTRATION/HANDLING
PHARMACOKINETICS
PO
Readily absorbed following PO admin- • Give without regard to food. May ad-
istration. Metabolized in liver, primar- minister with milk or food if GI upset
ily through oxidation. Protein binding: occurs.
V 98%. Peak plasma concentration: 7–11
hrs. Steady state reached within 2 wks. INDICATIONS/ROUTES/DOSAGE
Excreted in urine (59%), feces (26%). Major Depressive Disorder
Half-life: 66 hrs. PO: ADULTS/ELDERLY: Initially, 10 mg once
daily. May increase to 20 mg as tolerated.
LIFESPAN CONSIDERATIONS
Maintenance: 5–20 mg once daily.
Pregnancy/Lactation: May cause fetal
harm when administered in third tri- Dose Modification
mester. Unknown if distributed in breast Concomitant use of strong CYP2D6
milk. Exposed neonates are at increased inhibitors: Reduce dose by half of in-
risk of apnea, cyanosis, prolonged hos- tended therapy. Maximum: 10 mg once
pitalization, pulmonary hypertension, daily. Concomitant use of strong CYP

underlined – top prescribed drug


vortioxetine 1235
inducers: If coadministered for more than NURSING CONSIDERATIONS
14 days, consider increasing vortioxetine
dose. Maximum: Do not exceed more than BASELINE ASSESSMENT
3 times original dose. CYP2D6 poor me- Obtain baseline electrolytes. Note serum
tabolizers: Maximum: 10 mg once daily. sodium level. Assess appearance, be-
havior, speech pattern, level of interest,
Discontinuation mood. Screen for history of bipolar disor-
Gradually taper dose to minimize inci- der, bleeding events, SIADH, prior allergic
dence of withdrawal symptoms and to al- reactions to drug class. Receive full medi-
low detection of re-emerging symptoms. cation history including herbal products.
Dosage in Renal Impairment INTERVENTION/EVALUATION
No dose adjustment. Monitor serum sodium levels. Screen
Dosage in Hepatic Impairment
for signs of SIADH (confusion, sei-
Mild to moderate impairment: No
zures). Offer emotional support. Assess
dose adjustment. Severe impairment: mental status for depression, suicidal
Not recommended. ideation (esp. during first few mos of
therapy or with dosage change), anxi-
SIDE EFFECTS ety, social function. Monitor daily pat-
Frequent (32%–22%): Nausea, sexual dys-
tern of bowel activity, stool consistency.
function. Occasional (10%–3%): Diarrhea, Assist with ambulation if dizziness oc-
dizziness, dry mouth, constipation, vomit- curs. Monitor pt for symptoms of se-
ing, flatulence, abnormal dreams, pruritus. rotonin syndrome, mania/hypomania.
Offer antiemetic for nausea, vomiting.
ADVERSE EFFECTS/TOXIC Monitor for allergic reactions.
REACTIONS PATIENT/FAMILY TEACHING
Life-threatening serotonin syndrome may • Dry mouth may be relieved with
include mental status changes (agita- sugarless gum, sips of water. • Re-
tion, hallucinations, delirium, coma), port neurologic changes: confusion,
autonomic instability (tachycardia, la- excessive talking, hallucinations, head-
bile blood pressure, dizziness, sweating, ache, hyperactivity, insomnia, racing
flushing, hyperthermia), neuromuscular thoughts, seizure-like activity, tremors;
symptoms (tremor, rigidity, myoclonus sexual dysfunction; fever; or any type
[localized muscle twitching], hyperac- of allergic reaction. • Avoid tasks
tive reflexes, incoordination), seizures, that require alertness, motor skills un-
GI symptoms (nausea, vomiting, diar- til response to drug is established
rhea). May increase risk of bleeding (may cause dizziness, drowsi-
events such as ecchymosis, hematoma, ness). • Take with food if
epistaxis (nosebleed), petechiae. Mania/ nausea occurs. • Report pregnancy.
hypomania may indicate baseline bipolar V
• Avoid alcohol. • Do not take OTC
disorder. Syndrome of inappropriate an- medications such as aspirin or ibupro-
tidiuretic hormone (SIADH), also known fen without consulting physi-
as water intoxication or dilutional hypo- cian. • Immediately report thoughts
natremia, may induce seizures, coma, or of suicide, self-destructive behavior, or
death. Angioedema, dyspnea, rash may in- violence. • Sexual dysfunction such
dicate allergic reaction. May increase risk as inability to reach orgasm, difficulty
of suicidal ideation and behavior once maintaining an erection, or lack of
treatment is therapeutic. May alter sexual sexual drive may occur. • Do not
drive, ease of arousal, ease of reaching suddenly stop treatment. Dose must be
orgasm, or cause erectile dysfunction in gradually reduced over time.
men or decreased lubrication in women.
Canadian trade name Non-Crushable Drug High Alert drug
1236 warfarin
lumbar block anesthesia or traumatic sur-
warfarin gery, eclampsia /preeclampsia. Cautions:
Active tuberculosis, acute infection, dia-
war-far-in betes, heparin-induced thrombocytopenia
(Coumadin, Jantoven) and deep vein thrombosis, pts at risk for
j BLACK BOX ALERT jMay hemorrhage, moderate to severe renal
cause major or fatal bleeding. Risk impairment, moderate to severe hyperten-
factors include history of GI bleed- sion, thyroid disease, polycythemia vera,
ing, hypertension, cerebrovascular
disease, heart disease, malignancy, vasculitis, open wound, menstruating and
trauma, anemia, renal insufficiency, postpartum women, indwelling catheters,
age 65 yrs and older, high anticoag- trauma, prolonged dietary deficiencies,
ulation factor (INR greater than 4). disruption of GI normal flora, history of
Consider cardiac/hepatic function, peptic ulcer disease, protein C deficiency,
age, nutritional status, concurrent
medications, risk of bleeding when elderly.
dosing warfarin. Genetic variations
have been identified as factors as- ACTION
sociated with dosage and bleeding Interferes with hepatic synthesis of vita-
risk. Genotyping tests are available. min K–dependent clotting factors, result-
Do not confuse Coumadin with ing in depletion of coagulation factors II,
Kemadrin, or Jantoven with VII, IX, X. Therapeutic Effect: Prevents
Janumet or Januvia. further extension of formed existing clot;
uCLASSIFICATION
prevents new clot formation, secondary
thromboembolic complications.
PHARMACOTHERAPEUTIC: Vitamin K
antagonist. CLINICAL: Anticoagulant. PHARMACOKINETICS
Route Onset Peak Duration
USES PO 1.5–3 days 5–7 days 2–5 days
Prophylaxis, treatment of thromboem- Well absorbed from GI tract. Protein
bolic disorders and embolic complica- binding: 99%. Metabolized in liver. Pri-
tions arising from atrial fibrillation or marily excreted in urine. Not removed by
valve replacement. Risk reduction of hemodialysis. Half-life: 20–60 hrs.
systemic embolism following MI (e.g., re-
current MI, stroke). OFF-LABEL: Adjunct LIFESPAN CONSIDERATIONS
treatment in transient ischemic attacks. Pregnancy/Lactation: Contraindicated
in pregnancy (fetal, neonatal hemor-
PRECAUTIONS rhage, intrauterine death). Crosses pla-
Contraindications: Hypersensitivity to war­ centa; is not distributed in breast milk.
farin. Hemorrhagic tendencies (e.g., cere- Children: More susceptible to effect.
bral aneurysms, bleeding from GI tract), Elderly: Increased risk of hemorrhage;
recent or potential surgery of eye or CNS, lower dosage recommended.
W neurosurgical procedures, open wounds,
severe uncontrolled or malignant hyper- INTERACTIONS
tension, spinal puncture procedures, un- DRUG: Amiodarone, azole antifun­gals
controlled bleeding, ulcers, unreliable or (e.g., fluconazole), cimetidine, disulfi-
noncompliant pts, unsupervised pts, blood ram, sulfamethoxazole-trimethoprim,
dyscrasias, pericarditis or pericardial effu- levothyroxine, metroNIDAZOLE,
sion, pregnancy (except in women with NSAIDs (e.g., ibuprofen, ketorolac,
mechanical heart valves at high risk for naproxen), omeprazole, platelet ag-
thromboembolism), bacterial endocardi- gregation inhibitors (e.g., clopido-
tis, ­threatened abortion. Major regional grel), salicylates (e.g., aspirin), throm-

underlined – top prescribed drug


warfarin 1237
bolytic agents (e.g., alteplase), thyroid ADVERSE EFFECTS/TOXIC
hormones (e.g., levothyroxine), may REACTIONS
increase effect. CYP3A inducers (e.g., Bleeding complications ranging from
carBAMazepine, phenytoin, rifAMPin), local ecchymoses to major hemorrhage
nafcillin, oral contraceptives, sucral- (intracranial hemorrhage, GI /GU/nasal /
fate, vitamin K may d­ecrease effects. oral /rectal bleeding) may occur. Hepa-
HERBAL: Herbals with anticoagulant/ totoxicity, blood dyscrasias, necrosis,
antiplatelet properties (e.g., garlic, vasculitis, local thrombosis occur rarely.
ginger, ginkgo biloba), fenugreek, Antidote: Vitamin K. Amount based on
glucosamine may increase risk of bleed- INR, significance of bleeding. Range:
ing. FOOD: Foods rich in vitamin K 2.5–10 mg given orally or slow IV infu-
(e.g., spinach, brussels sprouts, meat) sion (see Appendix J for dosage).
may decrease effect. Cranberry juice may
increase effect. LAB VALUES: None known. NURSING CONSIDERATIONS
AVAILABILITY (Rx) BASELINE ASSESSMENT
1 mg, 2 mg,
Tablets: (Coumadin, Jantoven): Cross-check dose with co-worker. Obtain
2.5 mg, 3 mg, 4 mg, 5 mg, 6 mg, 7.5 mg, CBC, PT/INR before administration and
10 mg. daily following therapy initiation. When
stabilized, follow with INR determina-
ADMINISTRATION/HANDLING tion q4–6wks. Obtain genotyping prior to
PO initiating therapy if available. Screen for
• Give without regard to food. Give with major active bleeding. Question recent
food if GI upset occurs. • Give at same history of bleeding, recent trauma, surgi-
time each day. cal procedures, epidural anesthesia.

INDICATIONS/ROUTES/DOSAGE INTERVENTION/EVALUATION

b ALERT c Initial dosing must be indi- Monitor INR diligently. Assess CBC for
vidualized. anemia; urine/stool for occult blood.
Be alert to complaints of abdominal /
Anticoagulant back pain, severe headache, confusion,
PO: ADULTS, ELDERLY: Initially, 2–5 mg / seizures, hemiparesis, aphasia (may be
daily for 2 days or 5–10 mg daily for 1–2 sign of hemorrhage). Decrease in B/ P,
days, adjusting the dose based on INR increase in pulse rate may be sign of
results. Usual maintenance dose: 2–10 hemorrhage. Question for increase in
mg/day, but may vary outside these guide- amount of menstrual discharge. Assess
lines. CHILDREN: Initially, 0.2 mg/kg/day. peripheral pulses; skin for ecchymoses,
Maximum: 10 mg. Maintenance: Ad- petechiae. Check for excessive bleeding
just based on INR. from minor cuts, scratches. Assess gums
for erythema, gingival bleeding.
Dosage in Renal/Hepatic Impairment
No dose adjustment. Closely monitor PATIENT/FAMILY TEACHING
• Take medication at same time each W
INR.
day. • Blood levels will be monitored
SIDE EFFECTS routinely. • Do not take, discontinue any
Occasional: GI distress (nausea, anorexia, other medication except on advice of phy-
abdominal cramps, diarrhea). Rare: Hy- sician. • Avoid alcohol, aspirin, drastic
persensitivity reaction (dermatitis, urti- dietary changes. • Consult with physi-
caria), esp. in those sensitive to aspirin. cian before surgery, dental work. • Urine
may become red-orange. • Falls, subtle

Canadian trade name Non-Crushable Drug High Alert drug


1238 warfarin
injuries, esp. head or abdominal trauma, medication without physician approval
can be life-threatening. • Report bleed- (may interfere with platelet aggrega-
ing, bruising, red or brown urine, black tion). • Seek immediate medical atten-
stools. • Use electric razor, soft tooth- tion for stroke-like symptoms (confusion,
brush to prevent bleeding. • Report difficulty speaking, headache, one-sided
coffee-ground vomitus, blood-tinged mu- weakness); bloody stool or urine.
cus from cough. • Do not use any OTC

underlined – top prescribed drug


zafirlukast 1239
INTERACTIONS
zafirlukast DRUG: Erythromycin, theophylline may
decrease concentration/effect. May
za-fir-loo-kast increase effects of warfarin (increases
(Accolate) INR). HERBAL: None significant. FOOD:
Do not confuse Accolate with Food decreases bioavailability by 40%.
Accupril, Accutane, or Aclovate. LAB VALUES: None significant.
uCLASSIFICATION
AVAILABILITY (Rx)
PHARMACOTHERAPEUTIC: Leuko- Tablets: 10 mg, 20 mg.
triene receptor antagonist. CLINI-
CAL: Antiasthma. ADMINISTRATION/HANDLING
PO
USES • Give 1 hr before or 2 hrs after meals.
Prophylaxis, chronic treatment of bron- INDICATIONS/ROUTES/DOSAGE
chial asthma in adults and children 5 yrs Bronchial Asthma
and older. OFF-LABEL: Chronic urticaria. PO: ADULTS, ELDERLY, CHILDREN 12 YRS
AND OLDER: 20 mg twice daily. CHILDREN
PRECAUTIONS
5–11 YRS: 10 mg twice daily.
Contraindications: Hypersensitivity to
zafirlukast. Hepatic impairment. Cau- Dosage in Renal Impairment
tions: Elderly pts. Not approved for acute No dose adjustment.
asthma attacks, status asthmaticus.
Dosage in Hepatic Impairment
ACTION Contraindicated.
Competitive antagonist of leukotriene
receptor. Leukotriene production and SIDE EFFECTS
receptor occupation are associated with Frequent (13%): Headache. Occasional
pathophysiology of asthma. Therapeu- (3%): Nausea, diarrhea. Rare (less than
tic Effect: Reduces airway edema, 3%): Generalized pain, asthenia, myalgia,
smooth muscle constriction; alters cel- fever, dyspepsia, vomiting, dizziness.
lular activity associated with inflamma-
tory process. Reduces signs/symptoms ADVERSE EFFECTS/TOXIC
of asthma. REACTIONS
Concurrent administration of inhaled
PHARMACOKINETICS corticosteroids increases risk of upper
Rapidly absorbed after PO administration respiratory tract infection.
(food reduces absorption). Protein bind-
ing: 99%. Metabolized in liver. Primarily NURSING CONSIDERATIONS
excreted in feces. Unknown if removed by BASELINE ASSESSMENT
hemodialysis. Half-life: 10 hrs.
Obtain medication history. Assess LFT.
LIFESPAN CONSIDERATIONS Auscultate lung sounds.
Z
Pregnancy/Lactation: Drug is distrib- INTERVENTION/EVALUATION
uted in breast milk. Do not administer to Monitor rate, depth, rhythm, type of
breastfeeding women. Children: Safety respiration; quality, rate of pulse. Assess
and efficacy not established in pts lung sounds for rhonchi, wheezing, rales.
younger than 5 yrs. Elderly: No age- Monitor LFT.
related precautions noted.

Canadian trade name Non-Crushable Drug High Alert drug


1240 zanamivir
PATIENT/FAMILY TEACHING LIFESPAN CONSIDERATIONS
• Increase fluid intake (decreases lung Pregnancy/Lactation: Unknown if
secretion viscosity). • Take as pre- drug crosses placenta or is distributed
scribed, even during symptom-free peri- in breast milk. Children: Safety and ef-
ods. • Do not use for acute asthma ficacy not established in pts younger than
­episodes. • Do not alter, stop other 7 yrs (treatment) or younger than 5 yrs
asthma medications. • Do not breastfeed. (prevention). Elderly: No age-related
• Report nausea, jaundice, abdominal precautions noted.
pain, flu-like symptoms, worsening of
asthma. INTERACTIONS
DRUG: May decrease levels/effect of in-
fluenza virus vaccine. HERBAL: None
significant. FOOD: None known. LAB
zanamivir VALUES: None significant.

zan-am-i-veer AVAILABILITY (Rx)


(Relenza Diskhaler) Powder for Inhalation: 5 mg/blister.
uCLASSIFICATION ADMINISTRATION/HANDLING
PHARMACOTHERAPEUTIC: Neu- Inhalation
raminidase inhibitor. CLINICAL: An- • Instruct pt to use Diskhaler device
tiviral, anti-influenza. provided, exhale completely; then, hold-
ing mouthpiece 1 inch away from lips,
USES inhale and hold breath as long as possi-
ble before exhaling. • Rinse mouth
Treatment of uncomplicated acute ill- with water immediately after inhalation
ness due to influenza virus A and B in (prevents mouth/throat dryness). •
adults, children 7 yrs and older who Store at room temperature.
have been symptomatic for less than
2 days. Prevention of influenza A and INDICATIONS/ROUTES/DOSAGE
B in adults and children 5 yrs and Treatment of Influenza Virus
older. Inhalation: ADULTS, ELDERLY, CHILDREN
PRECAUTIONS 7 YRS AND OLDER: 2 inhalations (one
5-mg blister per inhalation for total dose
Contraindications: Hypersensitivity to zana­ of 10 mg) twice daily (approximately 12
mivir. Cautions: Not recommended in re- hrs apart) for 5 days.
spiratory disease (e.g., COPD, asthma),
renal/hepatic impairment. Prevention of Influenza Virus
Inhalation: ADULTS, ELDERLY, CHILDREN
ACTION 5 YRS AND OLDER: 2 inhalations (10 mg)
Inhibits influenza virus enzyme neur- once daily for duration of exposure pe-
aminidase, essential for viral replication. riod (7 days for household exposure, 28
Therapeutic Effect: Prevents viral re- days for community exposure).
Z lease from infected cells.
Dosage in Renal/Hepatic Impairment
PHARMACOKINETICS No dose adjustment.
Systemically absorbed, approximately
4%–17%. Protein binding: less than 10%. SIDE EFFECTS
Not metabolized. Excreted unchanged in Occasional (3%–2%): Diarrhea, sinusitis,
urine. Half-life: 2.5–5.1 hrs. nausea, bronchitis, cough, dizziness,

underlined – top prescribed drug


zidovudine 1241
headache. Rare (less than 1.5%): Malaise, FIXED-COMBINATION(S)
fatigue, fever, abdominal pain, myalgia, Combivir: zidovudine/lamiVUDine (an
arthralgia, urticaria. antiviral): 300 mg/150 mg. Trizivir:
zidovudine/lamiVUDine/abacavir (an
ADVERSE EFFECTS/TOXIC
antiviral): 300 mg/150 mg/300 mg.
REACTIONS
May produce neutropenia. Broncho- uCLASSIFICATION
spasm may occur in those with history PHARMACOTHERAPEUTIC: Nucleo-
of COPD, bronchial asthma. Neuro- side reverse transcriptase inhibitors.
psychiatric events (e.g., confusion, CLINICAL: Antiretroviral.
seizures, hallucinations) have been
reported.
USES
NURSING CONSIDERATIONS Treatment of HIV infection in combina-
BASELINE ASSESSMENT tion with at least two other antiretroviral
Pts requiring an inhaled bronchodilator agents. Prevention of maternal/fetal HIV
at same time as zanamivir should use the transmission. OFF-LABEL: Prophylaxis in
bronchodilator before zanamivir admin- health care workers at risk for acquiring
istration. HIV after occupational exposure (part of
multidrug regimen).
INTERVENTION/EVALUATION
Provide assistance if dizziness occurs. PRECAUTIONS
Monitor daily pattern of bowel activity, Contraindications: Potentially life-threat-
stool consistency. ening allergic reactions to zidovudine or
its components. Cautions: Bone marrow
PATIENT/FAMILY TEACHING compromise, renal/hepatic dysfunction.
• Follow manufacturer guidelines for Combination with interferon with or
use of delivery device. • Avoid contact without ribavirin in HIV/hepatitis C virus
with those who are at high risk for influ- (HCV) co-infection.
enza. • Continue treatment for full
5-day course. • Doses should be evenly ACTION
spaced. • In pts with respiratory dis- Interferes with viral RNA-dependent DNA
ease, an inhaled bronchodilator should polymerase, an enzyme necessary for
be readily available. viral HIV replication. Therapeutic Ef-
fect: Slows HIV replication, reducing
progression of HIV infection.

zidovudine PHARMACOKINETICS
Rapidly, completely absorbed from GI
zye-doe-vue-deen tract. Protein binding: 25%–38%. Me-
(Retrovir) tabolized in liver. Crosses blood-brain
barrier and is widely distributed, includ-
j BLACK BOX ALERT j Neutro- ing to CSF. Primarily excreted in urine.
penia, severe anemia may occur. Z
Lactic acidosis, severe hepatomeg- Minimal removal by hemodialysis. Half-
aly with steatosis (fatty liver), in- life: 0.5–3 hrs (increased in renal im-
cluding fatalities, have occurred. pairment).
Symptomatic myopathy, myositis
associated with prolonged use. LIFESPAN CONSIDERATIONS
Do not confuse Retrovir with Pregnancy/Lactation: Unknown if
acyclovir or ritonavir. drug crosses placenta or is distributed

Canadian trade name Non-Crushable Drug High Alert drug


1242 zidovudine
in breast milk. Unknown if fetal harm heparin, LORazepam (Ativan), mor-
or effects on fertility can occur. Chil- phine, potassium chloride.
dren: No age-related precautions noted.
Elderly: Information not available. INDICATIONS/ROUTES/DOSAGE
HIV Infection
INTERACTIONS PO: ADULTS, ELDERLY: 300 mg q12h.
DRUG: May decrease therapeutic effect CHILDREN 4 WKS TO 18 YRS WEIGHING 30 KG
of cladribine. DOXOrubicin, ganci- OR MORE: 300 mg q12h. WEIGHING 9–29
clovir, interferons, valganciclovir- KG: 9 mg/kg q12h. WEIGHING 4–8 KG: 12
may increase adverse effects. HERBAL: mg/kg q12h. PREMATURE NEONATES,
None significant. FOOD: None known. GA 35 WKS OR MORE: 4 mg/kg q12h, in-
LAB VALUES: May increase mean cor- crease to 12 mg/kg q12h after 4 wks of
puscular volume (MCV). age. GA 30–34 WKS: 2 mg/kg q12h for 2
wks, then 3 mg/kg q12h, then 12 mg/
AVAILABILITY (Rx) kg q12h after 6–8 wks. GA LESS THAN 30
Capsules: (Retrovir): 100 mg. Injection WKS: 2 mg/kg q12h, then 3 mg/kg q12h
Solution: (Retrovir): 10 mg/mL. Syrup: at 4 wks of age, then 12 mg/kg q12h after
(Retrovir): 50 mg/5 mL. Tablets: 300 8–10 wks of age.
mg. IV: ADULTS, ELDERLY, CHILDREN
OLDER THAN 12 YRS: 1 mg/kg/dose
ADMINISTRATION/HANDLING q4h around the clock. CHILDREN 12
IV YRS AND YOUNGER, FULL-TERM NEO-
NATES: 3 mg/kg/dose q12h. OLDER
Reconstitution • Must dilute before THAN 4 WKS: Increase to 9 mg/kg/dose
administration. • Remove calculated q12h. PREMATURE NEONATES: 1.5–2.3
dose from vial and add to D5W to provide mg/kg/dose q12h based on gestation
concentration no greater than 4 mg/mL. at birth. 6–10 WKS: Increase to 9 mg/
Rate of administration • Infuse over kg/dose q12h.
1 hr. May infuse over 30 min in neonates.
Storage • After dilution, IV solution is Prevention of Maternal/Fetal HIV
stable for 24 hrs at room temperature; Transmission
48 hrs if refrigerated. • Use within 8 Note: Zidovudine should be given IV
hrs if stored at room temperature or 24 near delivery regardless of antepartum
hrs if refrigerated to minimize potential regimen or mode of delivery in women
for microbial-contaminated solu- with HIV RNA level greater than 1,000
tion. • Do not use if solution is discol- copies/mL (or unknown status). Other
ored or precipitate forms. antiretrovirals should be continued
orally. Zidovudine IV is not required in
PO pts receiving HIV therapy with HIV RNA
• Keep capsules in cool, dry place. Pro- level less than 1,000 copies/mL near de-
tect from light. • May administer with- livery.
out regard to food. • Space doses IV: DURING LABOR AND DELIVERY: 2 mg/kg
evenly around the clock. • Pt should loading dose, then IV infusion of 1 mg/
Z maintain an upright position when kg/hr until delivery. For scheduled cesar-
given medication to prevent esophageal ean section, begin IV zidovudine 3 hrs
ulceration. before surgery. NEONATAL: Begin 6–12
hrs after birth and continue for first 6
IV COMPATIBILITIES wks of life. Use IV route only until oral
Dexamethasone (Decadron), DOBUTa- therapy can be administered.
mine (Dobutrex), DOPamine (Intropin), PO: FULL-TERM INFANTS: 4 mg/kg/
dose q12h (IV: 3 mg/kg/dose q12h).

underlined – top prescribed drug


ziprasidone 1243
INFANTS 30–34 WKS’ GESTATION: 2 mg/ INTERVENTION/EVALUATION
kg/dose q12h; increase to 3 mg/kg/ Monitor CBC, reticulocyte count, CD4
dose at 2 wks of age (IV: 1.5 mg/kg/ cell count, HIV RNA plasma levels.
dose q12h; increase to 2.3 mg/kg/ Check for bleeding. Assess for head-
dose q12h at 2 wks of age). INFANTS ache, dizziness. Monitor daily pattern of
LESS THAN 30 WKS’ GESTATION: 2 mg/ bowel activity, stool consistency. Evalu-
kg/dose q12h. (IV: 1.5 mg/kg/dose ate skin for acne, rash. Be alert to de-
q12h.) velopment of opportunistic infections
(fever, chills, cough, myalgia). Monitor
Dosage in Renal Impairment I&O, serum renal function, LFT. Check
ADULTS, ELDERLY:CrCl less than 15 mL/ for insomnia.
min, including hemodialysis or peri-
toneal dialysis: PO: 100 mg q8h or PATIENT/FAMILY TEACHING
300 mg once daily. IV: 1 mg/kg q6–8hr. • Doses should be evenly spaced around
INFANTS OLDER THAN 6 WKS, CHILDREN, the clock. • Zidovudine is not a cure
ADOLESCENTS: GFR 10 mL/min/1.73m2 for HIV infection, nor does it reduce risk
or greater: No adjustment. GFR less of transmission to others. Acts to reduce
than 10 mL/min/1.73m2: Administer symptoms and slows or arrests progress
50% of dose q8h. of disease. • Do not take any medica-
tions without physician’s approval.
Dosage in Hepatic Impairment • Bleeding from gums, nose, rectum
No dose adjustment. may occur and should be ­reported to
SIDE EFFECTS physician immediately. • Blood counts
are essential because of bleeding poten-
Expected (46%–42%): Nausea, headache. tial. • Dental work should be done be-
Frequent (20%–16%): Abdominal pain, fore therapy or after blood counts return
asthenia, rash, fever, acne. Occasional to normal (often wks after therapy has
(12%–8%): Diarrhea, anorexia, malaise, stopped). • Inform physician if muscle
myalgia, drowsiness. Rare (6%–5%): Diz- weakness, difficulty breathing, headache,
ziness, paresthesia, vomiting, insomnia, inability to sleep, unusual bleeding, rash,
dyspnea, altered taste. signs of infection occur.
ADVERSE EFFECTS/TOXIC
REACTIONS
Anemia (occurring most commonly after
4–6 wks of therapy), granulocytopenia
are particularly significant in pts with
ziprasidone
pretherapy low baselines. Neurotoxicity zi-pras-i-done
(ataxia, fatigue, lethargy, nystagmus, sei- (Geodon, Zeldox )
zures) may occur.
j BLACK BOX ALERT jIncreased
risk of mortality in elderly pts with
NURSING CONSIDERATIONS dementia-related psychosis, mainly
BASELINE ASSESSMENT
due to pneumonia, HF.
Do not confuse ziprasidone with Z
Avoid drugs that are nephrotoxic, cyto- traZODone.
toxic, myelosuppressive; may increase
risk of toxicity. Obtain specimens for viral uCLASSIFICATION
diagnostic tests before starting therapy PHARMACOTHERAPEUTIC: Second-
(therapy may begin before results are generation (atypical) antipsychotic.
obtained). Check hematology reports for CLINICAL: Antipsychotic.
accurate baseline.

Canadian trade name Non-Crushable Drug High Alert drug


1244 ziprasidone

USES in breast milk. Children: Safety and


Treatment of schizophrenia, acute agita- ­efficacy not established. Elderly: No age-
tion in pts with schizophrenia. Treatment related precautions noted. Use caution.
of acute mania or mixed episodes associ-
INTERACTIONS
ated with bipolar disorder with or with-
out psychosis. Maintenance treatment of DRUG: Alcohol, other CNS depres-
bipolar disorder as adjunct to lithium or sants (e.g., LORazepam, mor-
valproic acid. OFF-LABEL: Major depres- phine, zolpidem) may increase
sive disorder (adjunct to antidepressants). CNS depression. CarBAMazepine
may decrease concentration. QT in-
PRECAUTIONS terval–prolonging medications
Contraindications: Hypersensitivity (e.g., amiodarone, azithromycin,
to ziprasidone. Conditions associated haloperidol, moxifloxacin) may in-
with risk of prolonged QT interval, crease risk of QT interval prolongation,
congenital long QT syndrome, con- cardiac arrhythmias. HERBAL: Herb-
current use of other QT-prolongation als with sedative properties (e.g.,
medications (e.g., amiodarone, moxi- chamomile, kava kava, valerian)
floxacin, tacrolimus, thioridazine). may increase CNS depression. FOOD: All
Uncompensated HF. Recent MI. Cau- foods enhance bioavailability. LAB VAL-
tions: Pts with bradycardia, hypoka- UES: May prolong QT interval. May in-
lemia, hypomagnesemia may be at crease serum glucose, prolactin levels.
greater risk for torsades de pointes. AVAILABILITY (Rx)
History of MI or unstable heart dis-
ease, seizures, cardiac arrhythmias, Capsules: 20 mg, 40 mg, 60 mg, 80
disorders in which CNS depression is a mg. Injection, Powder for Reconstitution:
feature; pts at risk for aspiration pneu- 20 mg.
monia, hypotension, suicide; elderly, ADMINISTRATION/HANDLING
diabetes, hepatic impairment, Parkin-
IM
son’s disease, pts with breast cancer or
other prolactin-dependent tumors. • Store vials at room temperature; pro-
tect from light. • Reconstitute each vial
ACTION with 1.2 mL Sterile Water for Injection to
Exact mechanism unknown. Antago- provide concentration of 20 mg/
nizes alpha-adrenergic, DOPamine, mL. • Reconstituted solution stable for
histamine, serotonin receptors; in- 24 hrs at room temperature or 7 days if
hibits reuptake of serotonin, norepi- refrigerated.
nephrine. Therapeutic Effect: Di- PO
minishes symptoms of schizophrenia, • Give with food containing at least 500
depression. calories (increases bioavailability).
PHARMACOKINETICS INDICATIONS/ROUTES/DOSAGE
Well absorbed after PO administration. b ALERT c Dosage greater than 80 mg
Food increases bioavailability. Protein twice daily is not recommended in most
Z binding: 99%. Metabolized in liver. Ex- pts. To discontinue therapy: Gradu-
creted in feces. Not removed by hemodial- ally discontinue to avoid withdrawal
ysis. Half-life: PO: 7 hrs; IM: 2–5 hrs. symptoms, minimize risk of relapses.
LIFESPAN CONSIDERATIONS Schizophrenia
Pregnancy/Lactation: Unknown if PO: ADULTS, ELDERLY: Initially, 20 mg
drug crosses placenta or is distributed twice daily with food. Titrate at intervals

underlined – top prescribed drug


ziv-aflibercept 1245
of no less than 2 days based on response INTERVENTION/EVALUATION
and tolerability. Maintenance: 40–80 Assess for therapeutic response (greater
mg twice daily. interest in surroundings, improved self-
care, increased ability to concentrate,
Acute Agitation (Schizophrenia) relaxed facial expression). Monitor
IM: ADULTS, ELDERLY: 10 mg q2h or 20 weight.
mg q4h. Maximum: 40 mg/day. Switch
to oral therapy as soon as possible. PATIENT/FAMILY TEACHING
• Avoid tasks that require alertness, mo-
Bipolar Disorder (Acute and Maintenance tor skills until response to drug is estab-
as Adjunct to Lithium or Valproate) lished. • Avoid alcohol. • Report
PO: ADULTS, ELDERLY (Acute): Initially, chest pain, shortness of breathing, irreg-
40 mg twice daily. May increase to 60–80 ular heartbeats, fainting, palpitations.
mg twice daily on second day of treat-
ment. Maintenance: 40–80 mg twice
daily.
Dosage in Renal Impairment
ziv-aflibercept
Oral: No dose adjustment. IM: Use cau-
tion. ziv-a-flib-er-sept
(Zaltrap)
Dosage in Hepatic Impairment j BLACK BOX ALERT jSevere,
Use caution. and sometimes fatal, hemorrhagic
events including GI hemorrhage
SIDE EFFECTS were reported in pts receiving
concomitant FOLFIRI therapy.
Frequent (30%–16%): Headache, drowsi- Do not initiate in pts with severe
ness, dizziness. Occasional: Rash, hemorrhage. Fatal GI perforation
orthostatic hypotension, weight gain, may occur. Discontinue treatment
in pts with impaired wound healing.
restlessness, constipation, dyspepsia. Withhold treatment for at least 4
Rare: Hyperglycemia, priapism. wks prior to elective surgery. Do not
resume treatment for at least 4 wks
ADVERSE EFFECTS/TOXIC after major surgery until wound is
REACTIONS fully healed.
Prolongation of QT interval (as seen on Do not confuse ziv-aflibercept
ECG) may produce torsades de pointes, a with abatacept, Aricept, or
form of ventricular tachycardia. Pts with etanercept.
bradycardia, hypokalemia, hypomagne- uCLASSIFICATION
semia are at increased risk.
PHARMACOTHERAPEUTIC: Vascular
NURSING CONSIDERATIONS endothelial growth factor (VEGF)
inhibitor. CLINICAL: Antineoplastic.
BASELINE ASSESSMENT
Assess pt’s behavior, appearance, emo-
tional status, response to environment, USES
speech pattern, thought content. ECG Treatment of metastatic colorectal Z
should be obtained to assess for QT pro- cancer (mCRC) (in combination with
longation before instituting medication. 5-fluorouracil, leucovorin, irinotecan
Blood chemistry for serum magnesium, [FOLFIRI]) in pts resistant to or has pro-
potassium should be obtained before be- gressed following an oxaliplatin-contain-
ginning therapy and routinely thereafter. ing regimen.

Canadian trade name Non-Crushable Drug High Alert drug


1246 ziv-aflibercept

PRECAUTIONS FOOD: None known. LAB VALUES: May


Contraindications: Hypersensitivity to ziv- increase serum ALT, AST, serum creatinine;
afilbercept. Cautions: Baseline hemato- urine protein. May decrease leukocytes, neu-
logic cytopenias, (neutropenia,

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