Aplastic Anemia Drug Drug Category Mechanism of Action

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Aplastic Anemia

Drug Antithymocyte Globulin (Thymogam)


Drug Category Immunosuppressant
Mechanism of Action A lymphocyte- selective immunosuppressant that
reduces the peripheral circulation and alters the
function of thymus- dependent T- lymphocytes. It
also directly stimulates the growth of
haematopoietic stem cells and release of
haematopoietic growth factors
Adverse Drug Reaction Infusion site reactions, infection , leucopenia,
thrombocytopenia, dyspnoea, hypotension,
hypertension, tachycardia, oedema, serum
sickness, abnormal hepatic or renal function tests.
Rarely, haemolysis.
Drug Interaction Concomitant administration of live vaccines may
cause uncontrolled viral replication in
immunosuppressed patients
Therapeutic Dose In combination with other immunosuppressants:
10-20 mg/ kg once daily for 8-14 consecutive
days, then every other day, if needed, up to a total
of 21 doses in 28 days
Dosage Regimen Infuse over at least 4 hours via an in-line filter
(0.2-1 micron). Premedicate with antihistamine,
antipyretic, and/ or corticosteroid.
Drug Preparation Intravenous

Megaloblastic Anemia

Drug Folic Acid Vitamin B12


Drug Category Vitamins

Mechanism of Action It is also essential in Cyanocobalamin is vital to


nucleoprotein synthesis, growth, hematopoiesis and
maintenance of erythropoiesis nucleoprotein and myelin
and stimulation of WBC and synthesis.
platelet production in folate-
deficiency anaemia.
Adverse Drug Reaction Cardiac disorders: Flushing. Renal impairment Hepatic
Gastrointestinal disorders: impairment
Anorexia, nausea, abdominal
distention, flatulence. Immune
system disorders: Allergic
reactions. Nervous system
disorders: Malaise. Respiratory,
thoracic and mediastinal
disorders: Bronchospasm. Skin
and subcutaneous tissue
disorders: Erythema, pruritus,
skin rash, hypersensitivity.
Drug Interaction May decrease concentration of Drug-drug. Aminoglycoside s,
phenytoin. Decreased aminosalicylic acid and its salts,
absorption with sulfasalazine anticonvulsants, cobalt
and triamterene. irradiation of the small bowel,
Chloramphenicol, methotrexate colchicine, extended- release
and co- trimoxazole. It may potassium preparations:
interfere with folate metabolism.
May enhance the efficacy of Drug-lifestyle. Alcohol use:
lithium. Decreases vitamin B12
absorption from GI tract.
Smoking: Increases vitamin B12
requirement.
Therapeutic Dose Oral: 5 mg daily forupto4 50-150 mcg daily.
months. Parenteral: Up to 1 mg
daily given via IM/IV/SC inj.
Dosage Regimen As oral solution:May increase to Administer oral vitamin B12 with
15 mg daily in malabsorption meals to increase absorption
states. Maintenance: 5mg every
1-7 days. As parenteral:
Maintenance: 0.4 mg daily.
Drug Preparation Oral & Parenteral. May be taken Oral. Should b e taken on an
with or without food. empty stomach

Idiopathic Thrombocytopenic Purpura

Drug Prednisone IV IG
Drug Category Corticosteroid Immunoglobulin
Mechanism of Action Prednisone is a synthetic Inactive auto- reactive T-cells by
corticosteroid with glucocorticoid competing for and interrupting
and anti- inflammatory activity. their interaction with antigen
presenting cells. The balance of
cytokines also appears to be
restored by IVIg, with studies
showing that IVIg contains
antibodies and antagonists to
pro- inflammatory cytokines.

Adverse Drug Reaction Adrenal suppression, Local reactions w/ pain &


suppression of hypothalamic- tenderness at the inj site;
pituitary-adrenal , left ventricular hypersensitivity; systemic
free wall rupture, visual reactions w/ fever, chills, facial
disturbances, open-angle flushing, headache & nausea.
glaucoma, increased intraocular
pressure, central serous
chorioretinopathy
Drug Interaction May reduce the hypoglycemic There are no known drug
effects of antidiabetics. interactions; however IVIG
Increased risk of arrhythmias should not be applied at the time
with digitalis glycosides. of attenuated live vaccinations
Increased risk of gastrointestinal or within the 3- month period
ulceration or haemorrhage with after the vaccine.
NSAIDs, salicylates. May Cause
additional increased intraocular
pressure with anticholinergic
agents
Therapeutic Dose Initially, 5-60 mg daily 400 mg/kg daily for 2-5
consecutive days
Dosage Regimen Dosage is individualised and 400 mg/kg daily for 2-5
adjusted according to the consecutive days. Alternatively,
disease being treated and 800-1,000 mg/ kg given on day
patient response. May consider 1 & repeated on day 3 if
alternate day therapy for long- necessary.
term treatment
Drug Preparation Oral. Should be taken with food IV. Do not administer IM or SC.
Risk of anaphylactic reactions in
patients w/ IgA deficiencies.

Cushing’s Syndrome

Drug Ketoconazole
Drug Category Antifungal
Mechanism of Action Ketoconazole is also a potent cortisol and
aldosterone synthesis inhibitor due to its ability to
block several CYP450 enzymes in the adrenal
glands.
Adverse Drug Reaction Adrenal suppression, QT prolongation, bone
fragility, abnormal LFTs, hypersensitivity reactions
(e.g. anaphylaxis, angioedema).
Drug Interaction Increased risk of hyperkalemia and hypotension
with eplerenone. Increased risk of hepatotoxicity
and QTc interval prolongation with telithromycin
and clarithromycin. May reduce absorption with
antacids, antimuscarinic s, PPIs, H2- receptor
antagonists.
Therapeutic Dose 400 mg to 600 mg
Dosage Regimen The dose is titrated until a level of 1,200 mg to
1,600 mg, divided into four equal doses, is
reached
Drug Preparation Oral. Should be taken with food

Thyroid Storm

Drug Propylthiouracil
Drug Category Antithyroid
Mechanism of Action Propylthiouracil interferes with the catalyst thyroid
peroxidase, therefore preventing iodine from
being oxidised in the thyroid gland which results
in diminished thyroid hormone synthesis
Adverse Drug Reaction Bleeding, hypoprothrombinemia, bone marrow
suppression (e.g. aplastic anaemia,
thrombocytopenia, leucopenia), exfoliative
dermatitis, fever, hypothyroidism, lupus-like
syndrome (e.g. splenomegaly), nephritis,
glomerulonephritis, interstitial pneumonitis.
Drug Interaction May potentiate the effect of oral anticoagulants.
Concomitant β-blockers, digoxin and theophylline
may require dosage adjustments according to
changes in patient’s thyroid status.
Therapeutic Dose 300 mg daily in 3 equally divided doses
Dosage Regimen Initially, 300 mg daily in 3 equally divided doses
with approx 8- hour intervals.
Maintenance: 50-150 mg daily usually continued
for 1-2 years. Adjust dose based on patient’s
tolerability, clinical response and thyroid status.
Drug Preparation Oral. Should be taken with food

DM Type 1

Drug Glulisine Glargine


Drug Category Insulin Insulin
Mechanism of Action Insulin glulisine is a rapid acting Insulin glargine, a long-acting
human insulin analog produced analog of human insulin,
by recombinant DNA technology. regulates carbohydrate, protein
and fat metabolism by inhibiting
hepatic glucose production and
lipolysis, and enhancing
peripheral glucose disposal.

Adverse Drug Reaction Hypoglycaemia, Inj site Hypoglycaemia; oedema;


reactions, lipodystrophy, local pruritus; rash; hypersensitivity
and systemic hypersensitivity reactions; lipoatrophy or
reactions. lipohypertrophy with SC Inj
(rotate Inj site).
Drug Interaction Possible absence of Effects may be increased by:
hypoglycemic warning oral antidiabetic agents, ACE
symptoms with β-blockers. inhibitors, disopyramide,
Decreased hypoglycemic effect fibrates, fluoxetine, MAOIs,
with corticosteroid propoxyphene, salicylates,
somatostatin analog (e.g.
octreotide), sulfonamide
antibiotics.
Therapeutic Dose Dose should be individualised According to requirements
and depends on patient's needs.
Dosage Regimen By Inj: Admin within 15 minutes Administer once daily at the
before a meal or within 20 same time each day. For insulin-
minutes after starting a meal into naive patients: May initiate with
the abdominal wall, thigh, or 10 IU once daily. Adjust
upper arm. By continuous subsequently based on
infusion: Admin into the response to achieve glycaemic
abdominal wall. To be used in targets. Usual range: 2-100 IU/
conjunction with a longer-acting day.
insulin or basal insulin analogue.
Inj site should be rotated from
one inj to the next.
Drug Preparation Subcutaneous. Should be taken Subcutaneous
with food. Administer w/in 15
min before a meal or w/in 20 min
after starting a meal.

Hirsutism and Satyriasis

Drug Cyproterone Acetate


Drug Category Steroidal antiandrogen
Mechanism of Action Cyproterone is a steroidal anti- androgen that also
has antigonadotropi c and progestogen- like
activity. Ethinylestradiol is a synthetic oestrogen
with similar effects as estradiol.
Adverse Drug Reaction Breakthrough bleeding and missed withdrawal
bleeding, amenorrhoea, increased risk of breast
cancer, meningioma, impaired lipid levels,
jaundice, pruritus associated with cholestasis
Drug Interaction CYP3A4 inducers may increase the risk of
breakthrough bleeding and decrease overall
efficacy.
Therapeutic Dose Cyproterone 2 mg and ethinylestradiol 0.035 mg
tab
Dosage Regimen For women with moderate to severe androgen-
dependent acne and/or hirsutism who desire an
oral contraceptive for birth control: 1 tab once
daily, exactly as directed from the blister pack.
Doses must be taken continuously at the same
time each day. Refer to individual product
guideline for detailed dosing instructions.
Drug Preparation Oral, May be taken with or without food.

Acromegaly (Gigantism)

Drug Octreotide
Drug Category Octapeptide
Mechanism of Action A synthetic analogue of somatostatin which
acts by suppressing basal and stimulated
secretion of growth hormone (GH). It also
suppresses LH response to gonadotrophin-
releasing hormone and reduces the
secretion of gastrin, vasoactive intestinal
peptide (VIP), insulin, glucagon, secretin,
motilin and pancreatic polypeptide.
Adverse Drug Reaction Local pain, stinging, tingling at site of inj;
anorexia, nausea, vomiting, abdominal pain,
bloating, flatulence, loose stools,
steatorrhoea; biliary tract abnormalities.
Hypoglycaemia and hyperglycaemia,
hypothyroidism, cardiac conduction
abnormalities, pancreatitis.
Drug Interaction Dosage adjustment of concurrent therapy
may be necessary with calcium channel
blockers, oral hypoglycemics, β-blockers,
diuretics. May increase concentration of
bromocriptine.
Potentially Fatal: Requirements of insulin
may be reduced requiring careful blood-
glucose monitoring. Reduction in
cyclosporine bioavailability and efficacy.
Therapeutic Dose Intramuscular
Following initial control with SC therapy: As a
depot preparation, initially 20 mg every 4 wk.
Adjust if required after 3 mth to 10-30 mg
every 4 wk. Max: 40 mg every 4 wk.
Dosage Regimen Subcutaneous
Adult: Initially 50 mcg tid, increased as
necessary to usual dose 100-200 mcg tid.
Max: 500 mcg tid.
Drug Preparation Intamuscular/Subcutaneous

Hyperaldosteronism (Conn’s Syndrome)

Drug Spironolactone
Drug Category Aldosterone receptor antagonist
Mechanism of Action A specific pharmacologic antagonist of
aldosterone, acting primarily through
competitive binding of receptors at the
aldosterone-dependent sodium-potassium
exchange site in the distal convoluted renal
tubule. Spironolactone causes increased
amounts of sodium and water to be excreted,
while potassium is retained
Adverse Drug Reaction Benign breast neoplasm in male;
agranulocytosis, leucopenia,
thrombocytopenia; electrolyte imbalance,
hyperkalemia; changes in libido, confusion;
dizziness; nausea, GI disturbances,
abnormal hepatic function; pruritus, rash,
urticaria, toxic epidermal necrolysis, Stevens-
Johnson syndrome, drug reaction w/
eosinophilia & systemic symptoms (DRESS),
alopecia, hypertrichosis; muscle spasms;
acute kidney injury; gynecomastia, breast
pain, menstrual disorder; malaise.
Drug Interaction Severe hyperkalemia w/ drugs known to
cause hyperkalemia. Additive effect w/ other
diuretics & antihypertensives. Reduce
vascular responsiveness to norepinephrine;
increase t½ of digoxin; enhance metabolism
of antipyrine; interfere w/ assays for plasma
digoxin conc. NSAIDs may attenuate the
natriuretic efficacy of diuretics. Hyperkalemic
metabolic acidosis w/ ammonium Cl or
cholestyramine. Decreased efficacy w/
carbenoxolone.
Therapeutic Dose Diagnosis & treatment
Long test: 400 mg/day for 3-4 wk.
Short test: 400 mg/day for 4 days.
Dosage Regimen Short-term pre-op treatment: 100-400 mg
daily in prep for surgery.
Drug Preparation Oral

Hypoparathyroidism

Drug Vitamin D and Calcium


Drug Category Calcium/Vitamins

Mechanism of Action Calcium salt can be used in the prevention


and treatment of calcium deficiency states. It
is also used as an adjunct in the prevention
and treatment of osteoporosis. Vitamin D3 is
a fat-soluble sterol. It is necessary for the
regulation and regulation of calcium and
phosphate homoeostasis and bone
mineralisation.
Adverse Drug Reaction Constipation, nausea, abdominal pain,
hypercalcaemia, hypercalciuria, headache,
muscle weakness.
Drug Interaction Reduced absorption of tetracyclines,
quinolones and oral bisphosphonates with
concurrent calcium use. Calcium absorption
may be reduced by corticosteroids.
Increased risk of hypercalcemia and
metabolic alkalosis with thiazide diuretics.
High blood calcium level may increase the
effect of cardiac glycosides. Reduced
erlotinib efficacy with calcium. Increased risk
of hypercalcemia with paricalcitol. Enzyme-
inducing antiepileptics increases the
metabolism of Vit D.
Therapeutic Dose Calcium (expressed in terms of elemental
calcium): 19-50 yr: 1000 mg/day and >50 yr:
1200 mg/day. Vitamin D3: 10 mcg daily. 20
Dosage Regimen mcg daily for patients with limited sunlight
exposure, low vitamin D diet or bedridden
elderly patients.
Drug Preparation Oral

Endometriosis

Drug Combined Oral Contraceptive Pills


Drug Category COC
Mechanism of Action Suppression of ovulation by inhibition of
gonadotropin-releasing hormone (GnRH),
luteinizing hormone (LH), follicle-stimulating
hormone (FSH) and the mid-cycle LH surge.
This effect is mediated by both the progestin
and estrogen component of the COC working
synergistically, but estrogen suppression of
FSH, which in turn prevents folliculogenesis,
is likely the most important mechanism
Adverse Drug Reaction GI and menstrual disturbances, wt gain, fluid
retention, acne, melasma, allergic skin
rashes, urticaria, mental depression, breast
changes, altered libido, drowsiness/
insomnia, hirsutism, alopecia, jaundice and
anaphylactoid reactions (rare).
Drug Interaction Cyclosporin (risk of toxicity).
Therapeutic Dose 1-2 mg/day.

Dosage Regimen

Drug Preparation Oral

Infertility (PCOS)

Drug Metformin
Drug Category Antidiabetic agent/Antihyperglycemic agent
Mechanism of Action An antihyperglycemic agent which improves
glucose tolerance by lowering both basal and
postprandial plasma glucose. It decreases
glucose production by inhibiting
gluconeogenesis and glycogenolysis.
Adverse Drug Reaction Lactic acidosis. Metformin decreases liver
uptake of lactate increasing lactate blood
levels which may increase the risk of lactic
acidosis.
Drug Interaction Increased risk of hypoglycaemia with insulin
and insulin secretagogues (e.g.
sulfonylurea). Increased risk of lactic acidosis
with carbonic anhydrase inhibitors (e.g.
acetazolamide, dichlorphenamide), NSAIDs,
and antihypertensive agents (e.g. ACE
inhibitors). Increased plasma concentration
and reduced clearance with OCT2 inhibitors
(e.g. cimetidine, dolutegravir, ranolazine,
trimethoprim, vandetanib, isavuconazole).
Therapeutic Dose Initially, 500 or 850 mg bid or tid, gradually
increase at intervals of at least 1 week
according to response. Max: 300 mg daily in
Dosage Regimen 3 divided doses

Drug Preparation Oral

Benign Prostatic Hypertrophy

Drug Tamsulosin
Drug Category Alpha blockers
Mechanism of Action An antagonist of α1-adrenoceptors, which
mediate smooth muscle tone in the prostate.
This leads to the relaxation of smooth muscle
in the bladder neck and prostate thereby
improving urine flow and reducing the
symptoms of benign prostatic hyperplasia
(BPH).
Adverse Drug Reaction 1st dose orthostatic hypotension, syncope,
floppy iris syndrome in cataract and
glaucoma surgery, hypersensitivity reactions,
MI exacerbations.
Drug Interaction Increased serum concentration with weak or
strong CYP3A4 inhibitors (e.g. cimetidine,
ketoconazole) and strong CYP2D6 inhibitors
(e.g. paroxetine). Decreased plasma levels
with furosemide. Increased elimination rate
with diclofenac and warfarin. Enhanced
hypotensive effect with PDE5 inhibitors. May
enhance the antihypertensive effect of other
α1-adrenoceptor blockers.
Therapeutic Dose 400 mcg once daily.

Dosage Regimen

Drug Preparation Oral

Postpartum Hemorrhage

Drug Oxytocin
Drug Category Oxytocic hormone
Mechanism of Action Activates GPCR at the uterus, which causes
an increase in intracellular Ca levels in
uterine myofibrils. Thus promoting uterine
contractions. Stimulates the upper segment
of the myometrium to contract rhythmically,
constricting spiral arteries and decreasing
blood flow through the uterus. It stimulates
the release of prostaglandins and
leukotrienes.
Adverse Drug Reaction Foetal distress, arrhythmias, hypotension,
myocardial ischaemia, peripheral
vasodilation, tachycardia, QT prolongation,
uterine hypertonicity, spasm, tetanic
contraction, disseminated intravascular
coagulation (DIC).
Drug Interaction Enhanced effect of prostaglandins. Reduced
therapeutic efficacy and increased risk of
hypotension with inhalation anaesthetics
(e.g. halothane, sevoflurane, desflurane,
cyclopropane). Enhanced effect of
vasoconstrictors and sympathomimetics.
Increased risk of arrhythmia with drugs that
may prolong QT interval.
Therapeutic Dose For induction of labor: 0.5-2 mU/min is
increased every 30-60 mins. Maximum 20
mU/min.
Dosage Regimen Prevention: 10 IU IM or 5 to 10 IU IV bolus
Treatment: 20 to 40 IU in 1L of 5% normal
saline, infuse 500 mL over 10 mins then 250
mL per hour
Drug Preparation Intramuscular/Intravenous

Tics (Gilles De La Tourette’s Syndrome)

Drug Pimozide
Drug Category Antipsychotic
Mechanism of Action A diphenylbutylpiperidine antipsychotic. It
blocks the dopaminergic receptors in the
CNS resulting in its characteristic neuroleptic
effects.
Adverse Drug Reaction Extrapyramidal symptoms including acute
dystonic reactions, akathisia,
pseudoparkinsonism, tardive dyskinesia;
venous thromboembolism, grand mal
convulsions, anticholinergic effects (e.g.
constipation, xerostomia, blurred vision,
urinary retention), CNS depression,
esophageal dysmotility or aspiration,
hyperprolactinaemia, impaired core body
temperature regulation.
Drug Interaction Increased CNS depression produced by
other CNS depressants (e.g. hypnotics,
sedatives, strong analgesics). May impair the
anti-Parkinson effects of levodopa. Increased
risk of extrapyramidal effects with anti-
emetics (e.g. metoclopramide). Increased
risk of CNS toxicity with sibutramine.
Enhanced hypotensive effect with Ca
channel blockers. May cause electrolyte
imbalance with diuretics (especially those
causing hypokalemia).
Therapeutic Dose Adult: In patients who have failed to respond
satisfactorily to standard treatment: Initially,
1-2 mg daily in divided doses, may be

1-2 mg daily in divided doses, may be


Dosage Regimen increased thereafter every other day. Max: 10
mg daily or 0.2 mg/kg daily.
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Elderly: Half the usual initial dose.
Drug Preparation Oral

Schizophrenia

Drug Haloperidol
Drug Category Antipsychotic
Mechanism of Action Haloperidol is a first-generation (typical
antipsychotic) which exerts its antipsychotic
action by blocking dopamine D2 receptors in
the brain.
Adverse Drug Reaction Extrapyramidal symptoms
(pseudoparkinsonism, akathisia, tardive
dyskinesia, dystonia), CNS dep[ression,
constipation, xerostomia, blurred vision,
urinary retention, neuroleptic malignant
syndrome, bronchopneumonia. Blood
dyscrasias, torsades de pointes, infection at
injection site, diarrhea, nausea, sialorrhea
Drug Interaction If haloperidol is used in combination with
other central nervous system depressants
such as sedatives, alcohol or narcotics, the
actions and side effects of these drugs such
as sedation and respiratory depression will
be enhanced. Haloperidol can decrease the
effects of the treatment levodopa, which is
used in Parkinson’s disease.Quinidine,
buspirone and fluoxetine increase the
plasma haloperidol level while
carbamazepine, phenobarbital and rifampin
decrease the plasma haloperidol level.
Therapeutic Dose PO Psychoses; Schizophrenia; Mania 0.5-5
mg 2-3 times/day. Maintenance: 3-10 mg/
day. Adjust dose according to response and
tolerability.

IM Psychoses; Schizophrenia 2-10 mg in


subsequent doses given as often as every 60
minutes until symptoms are controlled,
administer with a dosage interval of 4-8
hours. Adjust dose according to response
and tolerability. Max: 18 mg/day.

Dosage Regimen Intramuscular Psychoses, Schizophrenia


Adult: Initially, 2-10 mg in subsequent doses
given as often as every 60 minutes until
symptoms are controlled, administer with a
dosage interval of 4-8 hours. Adjust dose
according to response and tolerability. Max:
18 mg daily.

Oral Mania, Psychoses, Schizophrenia


Adult: 0.5-5 mg 2-3 times daily.
Maintenance: 3-10 mg daily. Adjust dose
according to response and tolerability
Child: Schizophrenia: 3-12 years Initially 0.5
mg daily, increased to 1-4 mg daily. Max: 6
mg daily 13-17 years 0.5 mg daily, increased
to 1-6 mg daily. Max: 10 mg daily.
Elderly: 0.5-2 mg 2-3 times daily. Adjust
dose according to response and tolerability.
Max: 20 mg/day in divided doses.
Drug Preparation Oral: 0.5, 1, 2, 5, 10, 20 mg tablets; 2 mg/ml
concentrate. Parenteral: 5 mg/ml for IM

Smoking Cessation

Drug Varenicline
Drug Category Smoking Cessation Aids
Mechanism of Action Blocks the ability of nicotine to activate α4β2
receptors and thus to stimulate the central
nervous mesolimbic dopamine system,
believed to be the neuronal mechanism
underlying reinforcement and reward
experienced upon smoking.
Adverse Drug Reaction Nausea, GI disturbances. Depression,
headaches, dizziness, somnolence, fatigue,
erythema multiforme, Stevens-Johnson
Syndrome
Drug Interaction Increased incidence of adverse effects
(nausea and vomiting) with transdermal
nicotine. Increased exposure wit cimetidine
Therapeutic Dose Adult: PO 500 mcg once daily on days 1-3
followed by 500 mcg twice a day for days
4-7. Maintenance dose (week 2-12): 1 mg
twice a day

Dosage Regimen 500 mcg once daily for the 1st 3 days,
followed by 500 mcg bid for the next 4 days.
Maintenance (week 2-12): 1 mg bid. Initiate
dose 1-2 weeks prior to target quit date; may
temporarily reduce dose to 500 mcg bid if
adverse effects are not tolerable. Usual
treatment duration: 12 week. May continue
for another 12 week to reduce relapse in
patients who have successfully quit after the
initial treatment course
Drug Preparation Oral

Absence Epilepsy

Drug Ethosuximide
Drug Category Antiseizure
Mechanism of Action Ethosuximide has an important effect on Ca
2+ currents, reducing the low-threshold (T-
type) current. This effect is seen at
therapeuti-cally relevant concentrations in
thalamic neurons. The T-type Ca 2+currents
are thought to provide a pacemaker current
in thalamic neurons responsible for
generating the rhythmic cortical discharge of
an absence attack. Inhibition of this current
could therefore account for the specific
therapeutic action of ethosuximide. A recently
described effect on inwardly rectifying K +
channels may also be significant.
Adverse Drug Reaction Mental depression with suicidal thoughts,
SLE, drowsiness, dizziness, ataxia, irritability,
euphoria, lethargy, hiccups, microscopic
hematuria, myopia, urticarial, hirsutism,
blood dyscrasia, Stevens-Johnson
Syndrome, aplastic anemia
Drug Interaction Administration of ethosuximide with valproic
acid results in a decrease in ethosuximide
clearance and higher steady-state
concentrations owing to inhibition of
metabolism. No other important drug
interactions have been reported for the
succinimides.
Therapeutic Dose Therapeutic levels of 60–100 mcg/mL can be
achieved in adults with dosages of 750–1500
mg/d, although lower or higher dosages and
blood levels (up to 125 mcg/mL) may be
necessary and tolerated in some patients.
Ethosuximide has a linear relationship
between dose and steady-state plasma
levels. The drug might be administered as a
single daily dose were it not for its adverse
gastrointestinal effects; twice-a-day dosage
is common.
Dosage Regimen Oral Absence seizures
Adult: Initially, 500 mg daily in 2 divided
doses, may increase in increments of 250
mg at 4-7 days interval. Usual dose: 1-1.5 g
daily in 2 divided doses. Max: up to 2 g daily.
Child: Initially, 250 mg daily, may increase
gradually in small increments every few days
to a usual dose of 20 mg/kg daily. Max: 1 g
daily; > 6 yr Same as adult dose.
Drug Preparation Ethosuximide (generic, Zarontin) Oral: 250
mg capsules; 250 mg/5 mL syrup

Bipolar-Manic Disorder

Drug Lithium Bicarbonate


Drug Category Mood Stabilizer
Mechanism of Action Suppresses inositol signaling through
depletion of intracellular inositol and inhibits
glycogen synthase kinase-3 (GSK-3). It also
decreases norepinephrine release, and
increases serotonin synthesis. It prevents
mood swings between mania and depression
Adverse Drug Reaction Polydipsia, polyuria, decreases thyroid
function, edema, tremor, coma, seizure
Drug Interaction Renal clearance of lithium is reduced by
about 25% by diuretics and NSAIDs
Therapeutic Dose 0.6 – 1.2 mmol/L
Dosage Regimen 450-675 mg twice daily
Drug Preparation Oral: 150, 300, 600 mg capsules; 300 mg
tablets; 8 mEq/mL syrup
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Obsessive-Compulsive Disorder

Drug Fluoxetine
Drug Category Selective Serotonin Reuptake Inhibitor
Mechanism of Action Fluoxetine selectively inhibits serotonin
reuptake at the presynaptic neuronal
membrane leading to increased synaptic
concentrations of serotonin
Adverse Drug Reaction Insomnia, nervousness, tremor, restlessness,
headache, palpitations, blurred vision,
suicidal thoughts, behavior and serotonin
syndrome
Drug Interaction The therapeutic efficacy of Abaloparatide can
be decreased when used in combination with
Fluoxetine. The metabolism of
Acetohexamide can be decreased when
combined with Fluoxetine. Acetazolamide
may increase the central nervous system
depressant (CNS depressant) activities of
Fluoxetine. The serum concentration of
Acetaminophen can be increased when it is
combined with Fluoxetine.
Therapeutic Dose Adult: 20 mg once daily
Child: 10 mg daily
Dosage Regimen Adult: 20-60 mg daily. Maximum: 80 mg daily
in 2 divided doses
Child: 10 mg daily may be increased to 20
mg daily after 2 weeks. Maximum: 60 mg
daily
Drug Preparation Fluoxetine (generic, Prozac) Oral: 10, 20, 40
mg capsules; 10, 20 mg tablets; 20 mg/5
mL liquid Oral delayed-release (Prozac
Weekly): 90 mg capsules

Spinal Anesthesia (Knee Arthroplasty-No Cardiotoxicity)

Drug Bupivacaine
Drug Category local Anesthetics, Amides

Mechanism of Action Bupivacaine blocks the generation and the


conduction of nerve impulses by increasing
the threshold for electrical excitation in the
nerve, slowing the propagation of the nerve
impulse, and reducing the rate of rise of the
action potential. It also prevents
depolarization by binding to the intracellular
portion of sodium channels and blocking
sodium ion influx into neurons. The analgesic
effects of Bupivacaine are thought to
potentially be due to its binding to the
prostaglandin E2 receptors, E1, which
inhibits the production of prostaglandins.
Adverse Drug Reaction Bradycardia, hypotension, nausea, vomiting,
diplopia, neuropathy, peripheral nerve injury,
arachnoiditis, paresis and paraplegia, cardiac
arrhythmia
Drug Interaction Additive systemic toxic effect with other local
anesthetic or agents structurally related to
amide-type local anesthesia (lidocaine).
Increased myocardial depression with anti-
arrhythmics. Enhanced adverse effects with
hyaluronidase. Increased risk of adverse
effects with beta blockers and Ca-channel
blockers.
Therapeutic Dose Spinal block: 0.5% solution: 10-20 mg (2-4
mL)
Dosage Regimen Adult:
injectable solution
▪ 0.25% (Sensorcaine, Marcaine, generic)
▪ 0.5% (Sensorcaine, Marcaine, generic)
▪ Contains methylparaben
o injectable solution, preservative-free
▪ 0.25% (Sensorcaine-MPF, Marcaine,
generic)
▪ 0.5% (Sensorcaine-MPF, Marcaine,
generic)
▪ 0.75% (Sensorcaine-MPF, Marcaine
Preservative Free, generic)
o injection, spinal
▪ 0.75% (Sensorcaine MPF Spinal, Marcaine
Spinal, generic)
▪ Each 2-mL ampule contains 15 mg
bupivacaine HCL with 165 mg dextrose
o injection, single-dose vial
▪ 660mg/5mL (Posimir)

Child:
injectable solution
▪ 0.25% (Sensorcaine, Marcaine, generic)
▪ 0.5% (Sensorcaine, Marcaine, generic)
▪ Contains methylparaben
o injectable solution, preservative-free
▪ 0.25% (Sensorcaine-MPF, Marcaine,
generic)
▪ 0.5% (Sensorcaine-MPF, Marcaine,
generic)
▪ 0.75% (Sensorcaine-MPF, Marcaine
Preservative Free, generic)
Drug Preparation Parenteral: 0.25, 0.5, 0.75% for injection;
0.25, 0.5, 0.75% with 1:200,000 epinephrine

Myxedema Coma

Drug Levothyroxine (L-Thyroxine, T4)


Drug Category Thyroid Hormone

Mechanism of Action Levothyroxine is a synthetically prepared


levo-isomer of the thyroid hormone thyroxine
(T4, a tetra-iodinated tyrosine derivative) that
acts as a replacement in deficiency
syndromes such as hypothyroidism. T4
converted to its active metabolite, L-
triiodothyronine (T3). Thyroid hormones (T4
and T3) then bind to thyroid receptor proteins
in the cell nucleus and exert metabolic
effects: control of DNA transcription and
protein synthesis, involved in normal
metabolism, growth, and development,
promotes gluconeogenesis, increases
utilization and mobilization of glycogen
stores, stimulates protein synthesis, and
increases basal metabolic rate. Thus, by
acting as a replacement for natural thyroxine,
symptoms of thyroxine deficiency are
relieved.
Adverse Drug Reaction Where the individual tolerance limit for
levothyroxine is exceeded or in the case of
overdosage, it is possible for the following
clinical symptoms typical of hyperthyroidism
to occur, especially if the dose is increased
too quickly at the start of treatment: irregular
or rapid heart rate (tachycardia, palpitations,
arrhythmias such as atrial fibrillation and
extrasystoles), chest pain (angina pectoris),
headache, muscle weakness or cramps,
warmth and redness of the face (flushing),
fever, vomiting, disorders of menstruation,
pseudotumor cerebri (increased pressure in
the head with eye swelling), trembling,
restlessness, sleep disturbances, sweating
(hyperhidrosis), weight loss, diarrhea. In
such cases the daily dose should be reduced
or the medication withdrawn for several days.
Therapy may carefully be resumed once the
adverse effects have disappeared. In case of
hypersensitivity to any of the ingredients of
levothyroxine (Euthyrox), allergic reactions,
particularly of the skin, may occur. Cases of
angioedema (swelling of the face or throat)
have been reported.
At the first sign of any adverse drug reaction,
the patient must seek medical attention
immediately.

Drug Interaction A number of drugs have been shown to


impair the absorption of levothyroxine; these
drugs include calcium carbonate, aluminum-
containing antacids, sucralfate, iron
supplements, cholestyramine, sevelamer,
and, possibly, ciprofloxacin, raloxifene, and
orlistat. The therapeutic efficacy of
Levothyroxine can be increased when used
in combination with Acetylsalicylic acid. The
serum concentration of Tolvaptan can be
decreased when it is combined with
Levothyroxine.
Therapeutic Dose Levothyroxine IV— usually 300 – 400 mcg
initially, followed by 50 – 100 mcg orally daily
Dosage Regimen Mild Hypothyroidism
1.7 mcg/kg or 100-125 mcg PO qDay; not to
exceed 300 mcg/day

>50 years (or <50 yr with CV disease)


Usual initial dose: 25-50 mcg/day
May adjust dose by 12.5-25 mcg q6-8Week
>50 years with CV disease
Usual initial dose: 12.5-25 mcg PO qDay
May adjust dose by 12.5-25 mcg q4-6weeks
until patient becomes euthyroid and serum
TSH concentration normalized; adjustments
q6-8weeks also used
Dose range: 100-125 mcg PO qDay
Severe Hypothyroidism: Initial: 12.5-25 mcg
PO qDay. Adjust dose by 25 mcg/day
q2-4Week PRN
Subclinical Hypothyroidism: Initial: 1 mcg/kg
PO qDay may be adequate, OR If
replacement therapy not initiated, monitor
patient annually for clinical status
Myxedema Coma: 300-500 mcg IV once,
THEN 50-100 mcg qDay until patient is able
to tolerate oral administration; may consider
smaller doses in patients with cardiovascular
disease
Drug Preparation Oral: 25, 50, 75, 88, 100, 112, 125, 137, 150,
175, 200, 300 mcg
Tablets: 13, 25, 50, 75, 88, 100, 112, 125,
137, 150 mcg capsules
Parenteral: 200, 500 mcg per vial (100 mcg/
mL when reconstituted) for injection

Femoral to Popliteal By-pass Surgery (Cardiovascular Risk)

Drug Sevoflurane
Drug Category General Anesthesia

Mechanism of Action Sevoflurane induces a reduction in junctional


conductance by decreasing gap junction
channel opening times and increasing gap
junction channel closing times. Sevoflurane
also activates calcium dependent ATPase in
the sarcoplasmic reticulum by increasing the
fluidity of the lipid membrane.
Adverse Drug Reaction Cough, dizziness, drowsiness, increased
amount of saliva, shivering, vomiting,
headache
Drug Interaction Sevoflurane administration is compatible with
barbiturates, propofol, and other commonly
used intravenous anesthetics.
Benzodiazepines and opioids would be
expected to decrease the MAC of
sevoflurane in the same manner as with
other inhalational anesthetics. Sevoflurane
administration is compatible with
benzodiazepines and opioids as commonly
used in surgical practice. As with other
halogenated volatile anesthetics, the
anesthetic requirement for sevoflurane is
decreased when administered in combination
with nitrous oxide.
Therapeutic Dose Liquid: 250 ml for inhalation in 1.4% of
oxygen via closed method inhalation
Dosage Regimen Liquid: 100%
Anesthesia
o 12-25 years
▪ 2.6% in oxygen or 1.4% with 65% N2O/
35% oxygen
o 25-40 years
▪ 2.1% in oxygen or 1.1% with 65% N2O/
35% oxygen
o 40-60 years
▪ 1.7% in oxygen or 0.9% with 65% N2O/
35% oxygen
o 60-80 years
▪ 1.4% in oxygen or 0.7% with 65% N2O/
35% oxygen
Drug Preparation Liquid: 250 ml for inhalation

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