2 Chemotherapeutic Agents Lecture Part 2

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Notre Dame of Marbel University

College of Arts and Sciences


Nursing Department

Pyrazinamide
Description
a. The exact mechanism of action is unknown.
b. May be bacteriostatic or bactericidal, depending on its
concentration at the infection site and on the susceptibility
of the infecting organism
c. Used with at least 1 other antitubercular medication if
ineffectiveness of the primary medication(s) occurs
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

Pyrazinamide
Contraindications and cautions
a. Contraindicated in clients with hypersensitivity
b. Used with caution in clients with diabetes mellitus, renal impairment, or gout, and in
children
c. May decrease the effects of allopurinol, colchicine, and probenecid
d. Cross-sensitivity is possible with isoniazid, ethionamide, or nicotinic acid.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

Pyrazinamide
Side and adverse effects
a. Increases liver function tests and uric acid levels
b. Arthralgia, myalgia
c. Photosensitivity
d. Hepatotoxicity
e. Thrombocytopenia
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

Pyrazinamide
Nursing Interventions
a. Assess for hypersensitivity.
b. Evaluate CBC, liver function test results, and uric acid levels.
c. Observe for hepatotoxic effects; if they occur, withhold the medication and notify the
HCP.
d. Assess for painful or swollen joints.
e. Evaluate blood glucose level because diabetes mellitus may be difficult to control while
client is taking the medication.
f. To take the medication with food to reduce gastrointestinal distress
g. To avoid sunlight or ultraviolet light until photosensitivity is determined
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

Second-Line Medications for Tuberculosis


Rifabutin
Description
a. Inhibits mycobacterial DNA-dependent RNA polymerase and suppresses protein
synthesis
b. Used to prevent disseminated Mycobacterium avium complex (MAC) disease in clients
with advanced HIV infection
c. Used to treat active MAC disease and tuberculosis in clients with HIV infection
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

Second-Line Medications for Tuberculosis


Rifabutin
Cautions
a. Can affect blood levels of some medications, including oral contraceptives and some
medications used to treat HIV infection

b. A nonhormonal method of birth control should be used instead of an oral


contraceptive.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

Second-Line Medications for Tuberculosis


Rifabutin
Nursing Interventions

a. Observe for hepatotoxic effects; if they occur, withhold the medication and notify the HCP.
b. Assess for painful or swollen joints.
c. Assess for ocular pain or blurred vision.
d. Client education: That the medication can be taken without regard to food
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

Second-Line Medications for Tuberculosis


Rifapentine
Description: Used only for pulmonary tuberculosis

Cautions: Can affect blood levels of some medications, including oral


contraceptives and warfarin, and some medications used to treat HIV infection

Side and adverse effects


a. Red-orange–colored body secretions
b. Hepatotoxicity
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

Second-Line Medications for Tuberculosis


Rifapentine
Nursing Interventions
a. Obtain baseline liver function studies and assess throughout therapy.
b. Observe for hepatotoxic effects; if they occur, withhold the medication and
notify the HCP.
c. Client education:That the medication can be taken without regard to food
d. To avoid sunlight or ultraviolet light until photosensitivity is determined
e. That red-orange–colored body secretions may occur
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

Second-Line Medications for Tuberculosis


Capreomycin sulfate
Description
a. Mechanism of action is unknown.
b. Used to treat MDR-TB when significant resistance to other medications is expected
c. Administered intramuscularly

Contraindications and cautions


a. The risk of nephrotoxicity, ototoxicity, and neuromuscular blockade is increased with the use
of aminoglycosides or loop diuretics.
b. Used with caution in clients with renal insufficiency, acoustic nerve impairment, hepatic
disorder, myasthenia gravis, or parkinsonism
c. Not administered to clients receiving streptomycin
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

Second-Line Medications for Tuberculosis


Capreomycin sulfate
Side and adverse effects
a. Nephrotoxicity
b. Ototoxicity
c. Neuromuscular blockade
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

Second-Line Medications for Tuberculosis


Capreomycin sulfate
Nursing Interventions
a. Perform baseline audiometric testing.
b. Assess renal, hepatic, and electrolyte levels before administration.
c. Monitor intake and output.
d. Reconstituted medication may be stored for 48 hours at room temperature.
e. Administer intramuscularly, deep into a large muscle mass.
f. Rotate injection sites.
g. Observe injection site for redness, excessive bleeding, and inflammation.
h. Client education: Not to perform tasks that require mental alertness
i. To report any hearing loss, balance disturbances, respiratory difficulty, weakness, or signs of
hypersensitivity reactions
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
KETOLIDES
Therapeutic Actions and Indications
block protein synthesis within susceptible bacteria, leading to cell death
Telithromycin binds to specific ribosome subunits, leading to cell
death in susceptible bacteria, which includes several strains resistant
to other antibiotics.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
KETOLIDES
PHARMACOKINETICS
It is rapidly absorbed through the GI tract, reaching peak levels in 1 hour.
distributed, may cross the placenta, and does pass into breast milk.
metabolized in the liver with a half-life of 10 hours.
excreted in the urine and feces
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
KETOLIDES
PHARMACOKINETICS
It is rapidly absorbed through the GI tract, reaching peak levels in 1 hour.
distributed, may cross the placenta, and does pass into breast milk.
metabolized in the liver with a half-life of 10 hours.
excreted in the urine and feces
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
KETOLIDES
CONTRAINDICATION AND CAUTIONS:
known allergy to any component of the drug or to macrolide antibiotics
known congenital prolonged QT interval, bradycardia, or any proarrhythmic
condition
with myasthenia gravis, which is a black box warning with this drug
Use with caution in cases of renal or hepatic impairment
Use with caution with pregnant and lactating patients
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
KETOLIDES
ADVERSE EFFECTS:
GI tract: nausea, vomiting, taste alterations, and the potential for
pseudomembranous colitis.
Superinfections
Serious hypersensitivity reactions, including anaphylaxis
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
LINCOSAMIDES
Therapeutic Actions and Indications
react at almost the same site in bacterial protein synthesis
These drugs are used in the treatment of severe infections when a less-toxic
antibiotic cannot be used.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
LINCOSAMIDES
PHARMACOKINETICS
are rapidly absorbed from the GI tract or from IM injections
metabolized in the liver and excreted in the urine and feces.
cross the placenta and enter breast milk
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
LINCOSAMIDES
CONTRAINDICATIONS AND CAUTIONS
with caution in patients with hepatic or renal impairment,
Use during pregnancy and lactation only if the benefit clearly outweighs the risk
to the fetus or neonate
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
LINCOSAMIDES
ADVERSE EFFECTS:
with caution in patients with hepatic or renal impairment,
Use during pregnancy and lactation only if the benefit clearly outweighs the risk
to the fetus or neonate
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
LIPOGLYCOPEPTIDES (TELEVANCIN)
Therapeutic Actions and Indications
are semisynthetic derivatives of vancomycin
They inhibit bacterial cell wall synthesis by interfering with the polymerization
and cross-linking of peptidoglycans.
They bind to the bacterial membrane and disrupt the membrane barrier function
causing bacterial cell death
It is only approved for use in treating complicated skin and skin-structure
infections in adults
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
LIPOGLYCOPEPTIDES (TELEVANCIN)
PHARMACOKINETICS
available as an IV drug only.
It is rapidly absorbed with peak levels occurring at the end of the infusion.
The drug is widely distributed, may cross the placenta, and may pass into breast
milk.
Its site of metabolism is not known; It has a half-life of 8 to 9 hours.
It is excreted in the urine.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
LIPOGLYCOPEPTIDES (TELEVANCIN)
CONTRAINDICATIONS AND CAUTIONS
contraindicated with known allergy to any component of the drug
Black Box Warning with pregnant and lactating patients.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
LIPOGLYCOPEPTIDES (TELEVANCIN)
ADVERSE EFFECTS:
nausea, vomiting, taste alterations, diarrhea, loss of appetite, and risk of C.
difficile diarrhea.
Nephrotoxicity
There is a risk of prolonged QTc interval.
A transfusion reaction called red man syndrome with flushing, sweating, and
hypotension can occur with rapid infusion.
Infusion site reactions with pain and redness.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
MACROLIDES
Therapeutic Actions and Indications
are antibiotics that interfere with protein synthesis. Macrolides include
erythromycin (Ery-Tab, Eryc, and others), azithromycin (Zithromax),
clarithromycin (Biaxin), and dirithromycin (Dynabac).
may be bactericidal or bacteriostatic, exert their effect by binding to the bacterial
cell membrane and changing protein
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
MACROLIDES
PHARMACOKINETICS
are widely distributed throughout the body; they cross the placenta and enter the
breast milk
absorbed in the GI tract
Erythromycin is metabolized in the liver, with excretion mainly in the bile to feces
Azithromycin and clarithromycin are mainly excreted unchanged in the urine,
making it necessary to monitor renal function
Dirithromycin is converted from the prodrug dirithromycin to erythromycylamine
in the intestinal wall and excreted through the feces
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
MACROLIDES
CONTRAINDICATIONS AND CAUTIONS:
contraindicated in patients with a known allergy to any macrolide
Ocular preparations are contraindicated for viral, fungal, or mycobacterial
infections of the eye
Use with caution in patients with hepatic dysfunction,renal disease, pregnant and
lactating women
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
MACROLIDES
ADVERSE EFFECTS:
abdominal cramping, anorexia, diarrhea, vomiting, and pseudomembranous
colitis.
Other effects include neurological symptoms such as confusion, abnormal thinking,
and uncontrollable emotions
hypersensitivity reactions ranging from rash to anaphylaxis
superinfections
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
MONOBACTAM (AZTREONAM)
Therapeutic Actions and Indications
aztreonam’s structure is unique, and little cross-resistance occurs.
It is effective against gram-negative enterobacteria and has no effect on gram-
positive or anaerobic bacteria.
disrupts bacterial cell wall synthesis, which promotes leakage of cellular contents
and cell death in susceptible bacteria
The drug is indicated for th treatment of urinary tract, skin, intra-abdominal, and
gynecological infections, as well as septicemia.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
MONOBACTAM (AZTREONAM)
PHARMACOKINETICS
Aztreonam is available for IV and IM use only
half-life is 1.5 to 2 hours.
The drug is excreted unchanged in the urine.
It crosses the placenta and enters breast milk
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
MONOBACTAM (AZTREONAM)
CONTRAINDICATIONS AND CAUTIONS
contraindicated with any known allergy to aztreonam.
Use with caution in patients with a history of acute allergic reaction to penicillins
or cephalosporins
caution with renal or hepatic dysfunction and in pregnant and lactating women
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
MONOBACTAM (AZTREONAM)
ADVERSE EFFECTS
The adverse effects associated are relatively mild.
Local GI effects include nausea, GI upset, vomiting, and diarrhea.
Hepatic enzyme elevations
Other effects include inflammation, phlebitis, and discomfort at injection sites, as
well as the potential for allergic response, including anaphylaxis.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

I. OTHER ANTIBIOTICS
NURSING IMPLEMENTATION:
Assess for possible contraindications or precautions
Check culture and sensitivity reports
Ensure that the patient receives the full course of the medication
Monitor the site of infection and presenting signs and symptoms
Provide small, frequent meals
Arrange for appropriate treatment of superinfection
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


An infection caused by a fungus is called a mycosis
Fungi differ from bacteria in that the fungus has a rigid
cell wall that is made up of chitin and various
polysaccharides and a cell membrane that contains
ergosterol.
resistant to antibiotics
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


AZOLE ANTIFUNGALS
THERAPEUTIC ACTIONS AND INDICATIONS
a large group of antifungals used to treat systemic and topical fungal infections
include fluconazole (Diflucan), itraconazole (Sporanox), ketoconazole (Nizoral),
posaconazole (Noxafi l), terbinafi ne (Lamisil), and voriconazole (Vfend).
bind to sterols and can cause cell death (a fungicidal effect) or interfere with cell
replication (a fungistatic effect)
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


AZOLE ANTIFUNGALS
PHARMACOKINETICS
Ketoconazole is absorbed rapidly from the GI tract, and metabolized in the liver and excreted through the
feces.
Fluconazole reaches peak levels within 1 to 2 hours after administration, excreted unchanged in the urine.
Itraconazole is slowly absorbed from the GI tract and is metabolized in the liver, excreted in the urine and
feces.
Posaconazole is given orally, has a rapid onset of action, metabolized in the liver and excreted in the feces.
Terbinafine is rapidly absorbed from the GI tract, extensively metabolized in the liver, and excreted in the
urine with a half-life of 36 hours.
Voriconazole reaches peak levels in 1 to 2 hours if given orally, and metabolized in the liver with a half-life
of 24 hours and is excreted in the urine.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


AZOLE ANTIFUNGALS
CONTRAINDICATIONS AND CAUTIONS:
Contraindicated with patients with hepatic failure
Use in caution for liver and renal impairment
Should not be used in pregnancy and lactating mothers
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


AZOLE ANTIFUNGALS
ADVERSE EFFECTS:
Many of the azoles are associated with liver toxicity
can cause severe effects on a fetus or a nursing baby.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


ECHINOCANDIN ANTIFUNGALS
Therapeutic Actions and Indications
Drugs in this class include anidulafungin, caspofungin, and micafungin.
work by inhibiting glucan synthesis.
Glucan is an enzyme that is present in the fungal cell wall but not in
human cell walls.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


2. ECHINOCANDIN ANTIFUNGALS
PHARMACOKINETICS
Anidulafungin is given as a daily IV infusion for at least 14 days.
metabolized by degradation and excreted in the feces
Caspofungin is available for IV use.
slowly metabolized in the liver and bound to protein and widely distributed
throughout the body
excreted through the urine.
Micafungin is an IV drug. It has a rapid onset
excreted in the urine..
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


2. ECHINOCANDIN ANTIFUNGALS
CONTRAINDICATIONS AND CAUTIONS:
Anidulafungin may cross the placenta and enter breast milk
should not be used by pregnant or lactating women.
Caution must be used in the presence of hepatic impairment
Caspofungin can be toxic to the liver;
embryotoxic in animal studies, great caution during pregnancy and lactation
Micafungin should be used during pregnancy and lactation only if the benefits clearly
outweigh the risks.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


2. ECHINOCANDIN ANTIFUNGALS
ADVERSE EFFECTS:
hepatic toxicity
Potentially serious hypersensitivity reactions
bone marrow suppression
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


3. OTHER ANTIFUNGALS
Therapeutic Actions and Indications

These include amphotericin B (Abelcet, AmBisome, Amphotec), fl ucytosine (Ancobon),


griseofulvin (generic), and nystatin (Mycostatin, Nilstat).
work to cause fungal cell death or to prevent fungal cell reproduction
The drug binds to the sterols in the fungus cell wall, changing cell wall permeability AND
can lead to cell death (fungicidal effect) or prevent the fungal cells from reproducing
(fungistatic effect)
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


3. OTHER ANTIFUNGALS
PHARMAKOKINETICS

These include amphotericin B (Abelcet, AmBisome, Amphotec), fl ucytosine (Ancobon),


griseofulvin (generic), and nystatin (Mycostatin, Nilstat).
work to cause fungal cell death or to prevent fungal cell reproduction
The drug binds to the sterols in the fungus cell wall, changing cell wall permeability AND
can lead to cell death (fungicidal effect) or prevent the fungal cells from reproducing
(fungistatic effect)
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


3. OTHER ANTIFUNGALS
CONTRAINDICATIONS AND CAUTIONS

should not be used during pregnancy or lactation unless the benefits


clearly outweigh the potential risks.
used cautiously on patients with renal impairement
Patients who receive amphotericin B should not take other nephrotoxic drugs such as
nephrotoxic antibiotics or antineoplastics, cyclosporine, or corticosteroids unless
absolutely necessary because of the increased risk of severe renal toxicity.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


3. OTHER ANTIFUNGALS
ADVERSE EFFECTS
Hepatotoxicity
Neprotoxicity
Bone marrow suppression
Rash
GI irritation with nausea, vomiting, and potentially severe diarrhea,
anorexia and weight loss
pain at the injection site
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


3. OTHER ANTIFUNGALS
NURSING IMPLEMENTATION:
Assess the patient for contraindications or cautions
Evaluate renal and hepatic function tests
Administer the entire course of the drug
Monitor IV sites to ensure that phlebitis or infiltration
Report to a health care provider any of the following: sore throat, unusual
bruising and bleeding, or yellowing of the eyes or skin, all of which could
indicate hepatic toxicity
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


4. TOPICAL ANTIFUNGALS
DERMATOPHYTES -Fungi that cause mycoses
mycoses include tinea infections such as
athlete’s foot (tinea pedis),
jock itch (tinea cruris),
yeast infections of the mouth and vagina often caused by
Candida
Examples: ketoconazole ( Nizoral,), sertaconazole nitrate (Ertaczo),
sulconazole (Exelderm), terbinafine (Lamisil),
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


4. TOPICAL ANTIFUNGALS
Therapeutic Actions and Indications

work to alter the cell permeability of the fungus, causing prevention of


replica and fungal death
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


4. TOPICAL ANTIFUNGALS
PHARMACOKINETIC

These drugs are not absorbed systemically and do not undergo


metabolism or excretion in the body.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


4. TOPICAL ANTIFUNGALS
CONTRAINDICATIONS AND CAUTIONS

contraindications are limited to a known allergy to any of these drugs and


open lesions.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

III. ANTI-FUNGAL AGENTS


4. TOPICAL ANTIFUNGALS
ADVERSE EFFECTS
local effects include irritation, burning, rash, and swelling.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

J. ANTI-FUNGAL AGENTS
4. TOPICAL ANTIFUNGALS
NURSING IMPLEMENTATION:
Topical creams and lotions should be gently rubbed into the affected area
after it has been cleansed with soap and water and patted dry
Advise the patient to stop the drug if a severe rash occurs
The importance of not placing drugs near open wounds or active lesions
because these agents are not intended to be absorbed systemically.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


Protozoa—single-celled organisms that pass through several stages in their life cycles.
thrive in tropical climates, but may also survive and reproduce in any area where people
live in very crowded and unsanitary conditions.
protozoal infections can be caused by insect bites
malaria
trypanosomiasis
leishmaniasis) and
those that result from ingestion
amebiasis
giardiasis
trichomoniasis
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


MALARIA
is a parasitic disease through the bite of a female Anopheles mosquito, an insect that
harbors the protozoal parasite.
FOUR PROTOZOAL PARASITES:
Plasmodium falciparum is considered to be the most dangerous type of protozoan.
Plasmodium vivax causes a milder form of the disease, which seldom results in
death.
Plasmodium malariae is endemic in many tropical countries and causes very mild
signs and symptoms in the local population.
Plasmodium ovale, which is rarely seen, seems to be in the process of being
eradicated.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


ANTI-MALARIALS
are usually given in combination form to attack the Plasmodium.
drugs can be:

schizonticidal -acting against the red-blood-cell phase of the life cycle,


gametocytocidal -acting against the gametocytes
sporontocidal - acting against the parasites that are developing in the mosquito,
schizonts as prophylactic or antirelapse agents -work against tissue .
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


ANTI-MALARIALS
Therapeutic Actions and Indications
Chloroquine is currently the mainstay of antimalarial therapy
directly toxic to parasites that absorb it; it is acidic, and it decreases the ability of the
parasite to synthesize DNA, leading to a blockage of reproduction.
Mefloquine increases the acidity of plasmodial food vacuoles, causing cell rupture and
death.
Primaquine disrupts the mitochondria of the Plasmodium, causes death of gametocytesan
d prevents other forms from reproducing.
Pyrimethamine is used in combination to suppress malaria; it acts by blocking the use of
folic acid in protein synthesis by the Plasmodium
Quinine inhibits nucleic acid synthesis, protein synthesis, and glycolysis in P. falciparum.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


ANTI-MALARIALS
PHARMACOKINETIC

Generally metabolized in the liver


Excreted in the urine
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


ANTI-MALARIALS
CONTRAINDICATIONS AND CAUTIONS:

allergy to any of these drugs;


liver disease
alcoholism
lactation
avoided during pregnancy
Use caution in patients with retinal disease
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


ANTI-MALARIALS
ADVERSE EFFECTS
Central nervous system (CNS) effects include headache and dizziness.
Immune reaction effects related to the release of merozoites fever, shaking, chills, and malaise
Nausea, vomiting,
dyspepsia
anorexia
Hepatic dysfunction
Dermatological effects include rash, pruritus, and loss of hair
Cinchonism (nausea, vomiting, tinnitus, and vertigo) may occur with high levels of quinine or
primaquine.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


ANTI-MALARIALS
NURSING IMPLEMENTATION:
Assess for contraindications or cautions: history of allergy to any of the
antimalarials
Perform ophthalmic and retinal examinations and auditory screening
Assess the patient’s liver function, including liver function tests
Administer the complete course of the drug
Take safety precautions, including changing position slowly and avoiding driving
and hazardous tasks, if CNS effects occur
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


OTHER PROTOZOAL INFECTIONS
Amebiasis,-an intestinal infection caused by Entamoeba histolytica, is often
known as amebic dysentery
Early signs of amebiasis include mild to fulminate diarrhea.
Two stages:
Cystic, dormant stage -the protozoan can live for long periods outside the
body or in the human intestine,
Trophozoite stage in the ideal environment—the human large intestine.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


OTHER PROTOZOAL INFECTIONS
Leishmaniasis is a disease caused by a protozoan that is passed from sand fl
ies to humans.
promastigote -fly injects an asexual form of this flagellated protozoan and
digested by human macrophages.
amastigotes - formed inside the macrophages as the promastigote divides.
can cause serious lesions in the skin, the viscera, or the mucous
membranes of the host.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


OTHER PROTOZOAL INFECTIONS
Trypanosomiasis is caused by infection with Trypanosoma.
Two parasitic protozoal species:
African sleeping sickness- caused by Trypanosoma brucei gambiense, (transmitted by the
tsetse fly)
invades the CNS, leading to an acute inflammation that results in lethargy, prolonged
sleep, and even death.

Chagas’ disease, which is caused by Trypanosoma cruzi


This protozoan results in a severe cardiomyopathy that accounts for numerous deaths
and disabilities in South American regions.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


OTHER PROTOZOAL INFECTIONS
Trichomoniasis -Trichomonas vaginalis, is a common cause of vaginitis.
This infection is usually spread during sexual intercourse .
In women, causes reddened, inflamed vaginal mucosa, itching, burning, and a yellowish-green discharge

Giardiasis- caused by Giardia lamblia, which survive outside the body and allow transmission through
contaminated water or food, and trophozoites.
Diarrhea, rotten egg–smelling stool, and pale and mucus-filled stool are commonly seen.

Pneumocystis jiroveci Pneumonia -Pneumocystis jiroveci is an endemic protozoan that does not usually cause
illness in humans.
immune system becomes suppressed because of acquired immune deficiency syndrome (AIDS) or AIDS-related
complex
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


OTHER PROTOZOAL AGENTS
Other antiprotozoals include
atovaquone (Mepron)
metronidazole (Flagyl, MetroGel, Noritate)
nitazoxanide (Alinia)
pentamidine (Pentam 300, NebuPent)
tinidazole (Tindamax)
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


OTHER PROTOZOAL AGENTS
Therapeutic Actions and Indications

act to inhibit DNA synthesis in susceptible protozoa, interfering with the


cell’s ability to reproduce, subsequently leading to cell death.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


OTHER PROTOZOAL AGENTS
PHARMACOKINETIC

generally metabolized in the liver


excreted in the urine and feces
Pentamidine is readily absorbed through the lungs.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


OTHER PROTOZOAL AGENTS
CONTRAINDICATIONS AND CAUTIONS

allergy or hypersensitivity to any of these drugs


Use caution when administering these drugs to patients with CNS disease
and lactating women
The safety and efficacy of pentamidine in children have not been
established.
Tinidazole should never be combined with alcohol and should be used with
caution in patients with renal dysfunction
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


OTHER PROTOZOAL AGENTS
ADVERSE EFFECTS

CNS effects such as headache, dizziness, ataxia, loss of coordination, and


peripheral neuropathy
GI effects include nausea, vomiting, diarrhea, unpleasant taste (METALLIC),
cramps, and changes in liver function.
Superinfections
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

IV. ANTI-PROTOZOAL DRUGS


OTHER PROTOZOAL AGENTS
NURSING IMPLEMENTATION

Assess for contraindications and cautions: history of allergy to any of the


antiprotozoals
Evaluate the CNS to check refl exes and muscle strength
Evaluate liver function, including liver function tests
Report severe GI problems and interference with nutrition; fever and chills,
which may indicate the presence of a superinfection, and dizziness,
unusual fatigue, or weakness, which may indicate CNS effects
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

V. ANTI-HELMINTIC DRUGS
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

V. ANTI-HELMINTHIC DRUGS
HELMINTHIC INFECTIONS
infections in the gastrointestinal (GI) tract or other tissues due to worm
infestation
two types:
the nematodes (or roundworms)
the platyhelminths (or flatworms)
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

V. ANTI-HELMINTHIC DRUGS
INTESTINE-INVADING WORM INFECTIONS
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

V. ANTI-HELMINTHIC DRUGS
TISSUE-INVADING WORM INFECTIONS
Trichinosis is the disease caused by ingestion of the encysted larvae of the roundworm,
Trichinella spiralis, in undercooked pork.
They can penetrate skeletal muscle and can cause an inflammatory reaction in cardiac
muscle and in the brain
Filariasis refers to infection of the blood and tissues of healthy individuals by worm
embryos, which enter the body via insect bites.
This may lead to severe swelling of the hands, feet, legs, arms, scrotum, or breast—a
condition called elephantiasis.
Schistosomiasis - is a platyhelminthic infection by a fluke that is carried by a snail.
severe infestation may lead to abdominal pain and diarrhea, as well as blockage of blood
fl ow to areas of the liver, lungs, and CNS.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

V. ANTI-HELMINTHIC DRUGS
act on metabolic pathways that are present in the invading worm but are absent or
significantly different in the human host.
include
albendazole (Albenza)
ivermectin (Stromectol)
mebendazole (Vermox)
praziquantel (Biltricide)
pyrantel (Antiminth, Pin-Rid, Pin-X, Reese’s Pinworm)
V. ANTI-HELMINTHIC DRUGS
Therapeutic Actions and Indications
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

V. ANTI-HELMINTHIC DRUGS
PHARMACOKINETIC
Mebendazole is not metabolized in the body, and most of it is excreted unchanged in the
feces. A small amount may be excreted in the urine.
Albendazole is poorly absorbed from the GI tract and metabolized in the liver and primarily
excreted in urine.
Ivermectin is readily absorbed from the GI tract. metabolized in the liver and excretion is
through the feces.
Praziquantel rapidly absorbed from the GI tract,metabolized in the liver and excretion
through the urine
Pyrantel is poorly absorbed, and most of the drug is excreted unchanged in the feces and
some found in the urine
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

V. ANTI-HELMINTHIC DRUGS
CONTRAINDICATIONS AND CAUTIONS
known allergy to any of these drugs
Pregnancy and lactation-Women of childbearing age should be advised to
use barrier contraceptives while taking these drugs.
Pyrantel has not been established as safe for use in children younger than 2
years
Use caution in the presence of renal or hepatic disease
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

V. ANTI-HELMINTIC DRUGS
ADVERSE EFFECTS

abdominal discomfort, diarrhea, or pain


headache and dizziness; fever, shaking, chills, and malaise
Renal failure and severe bone marrow depression are associated with
albendazole
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

V. ANTI-HELMINTIC DRUGS
NURSING IMPLEMENTATION
Assess for possible contraindications or cautions: history of allergy
Evaluate liver function and renal function tests
Proper hygiene and sanitation process are an important part in preventing
the spread of helminths, including good hand hygiene and preparation and
storage of food
Prevention is part of the treatment: laundering of bed linens, pajamas, and
underwear to destroy ova that are shed during the night; and disinfection of
toilet facilities at least daily and of bathroom floors.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

VI. ANTI-VIRAL AGENTS


Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

VI. ANTI-VIRAL AGENTS


virus particle is composed of a piece of DNA or RNA inside a protein.
replicates in the host cell.
When the host cell can no longer carry out its own metabolic functions
the host cell dies and releases the new viruses into the body.
Interferons - act to prevent the replication of that particular virus.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

VI. ANTI-VIRAL AGENTS


AGENTS FOR INFLUENZA A AND RESPIRATORY VIRUSES
Influenza A, B and RSV invade the respiratory tract and cause the
signs and symptoms of respiratory “flu.”
Agents for Influenza A and Respiratory Viruses
amantadine
oseltamivir
ribavirin
rimantadine
zanamivir
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

VI. ANTI-VIRAL AGENTS


AGENTS FOR INFLUENZA A AND RESPIRATORY VIRUSES
Therapeutic Actions and Indications
mechanism of action of drugs is not known
Oseltamivir is the only antiviral agent that is effective in treating H1N1
and avian flu.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

VI. ANTI-VIRAL AGENTS


AGENTS FOR INFLUENZA A AND RESPIRATORY VIRUSES
Pharmacokinetics
Generally absorbed in the GI and excreted through urine.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

VI. ANTI-VIRAL AGENTS


AGENTS FOR INFLUENZA A AND RESPIRATORY VIRUSES
Contraindications and Cautions:
with caution in patients who have any renal impairment
Embryotoxic - should be used during pregnancy and lactation only
if the benefi ts clearly outweigh the risks to the fetus or neonate.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

VI. ANTI-VIRAL AGENTS


AGENTS FOR INFLUENZA A AND RESPIRATORY VIRUSES
Adverse Effects:
light-headedness
dizziness, and insomnia
nausea
orthostatic hypotension
urinary retention
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

VI. ANTI-VIRAL AGENTS


AGENTS FOR INFLUENZA A AND RESPIRATORY VIRUSES
Nursing Implementation
Assess for contraindications or cautions eg. pregnancy
Assess for orientation and reflexes to evaluate any central nervous
system (CNS) effects of the drug
Start the drug regimen as soon after exposure to the virus as possible
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

VI. ANTI-VIRAL AGENTS


AGENTS FOR HERPES AND CYTOMEGALOVIRUS
Herpes viruses account for a broad range of conditions: cold sores,
encephalitis,shingles,genital infections

Cytomegalovirus (CMV) - different since it can affect the eye, respiratory tract,
and liver and reacts to many of the same drug.

acyclovir (Zovirax), cidofovir (Vistide), famciclovir (Famvir), foscarnet


(Foscavir), ganciclovir (Cytovene), valacyclovir (Valtrex), and valganciclovir
(Valcyte)
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

VI. ANTI-VIRAL AGENTS


AGENTS FOR HERPES AND CYTOMEGALOVIRUS
Therapeutic Actions and Indications
action prevents replication of the virus.
are indicated for treatment of the DNA viruses herpes simplex, herpes
zoster, and CMV.
very effective in immunocompromised individuals, such as patients with
AIDS, those taking immunosuppressants, and those with multiple
infections.
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

VI. ANTI-VIRAL AGENTS


AGENTS FOR HERPES AND CYTOMEGALOVIRUS
Pharmacokinetics
Most of the agents are readily absorbed and excreted through the
kidney and remained unchained in the urine
It crosses into breast milk
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

VI. ANTI-VIRAL AGENTS


AGENTS FOR HERPES AND CYTOMEGALOVIRUS
Adverse Effects
nausea and vomiting
headache,
depression
paresthesias,
neuropathy,
rash
hair loss
Renal dysfunction and renal failure
Notre Dame of Marbel University
College of Arts and Sciences
Nursing Department

VI. ANTI-VIRAL AGENTS


AGENTS FOR HERPES AND CYTOMEGALOVIRUS
Nursing Implementation
Assess for contraindications or cautions
Examine skin (color, temperature, and lesions)
Evaluate renal function tests
Administer the drug as soon as possible after the diagnosis has been made
Wear protective gloves when applying the drug topically
Provide the following patient teaching: Avoid sexual intercourse if genital herpes is
being treated because these drugs do not cure the disease

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