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chloroquine (Aralen)
MECHANISM OF ACTION
Chloroquine inhibits the action of heme polymerase in malarial trophozoites, preventing the conversion
of heme to hemazoin. Plasmodium species continue to accumulate toxic heme, killing the parasite.
Chloroquine passively diffuses through cell membranes and into endosomes, lysosomes, and Golgi
vesicles; where it becomes protonated, trapping the chloroquine in the organelle and raising the
surrounding pH. The raised pH in endosomes, prevent virus particles from utilizing their activity for
fusion and entry into the cell.
ADVERSE EFFECT
• headache nausea. loss of appetite. diarrhea. upset stomach. stomach pain. rash. itching
CONTRAINDICATIONS
NURSING CONSIDERATIONS
- Prophylaxis is not 100 per cent effective. It is important to inform travellers about mosquito bites and
taking drug regularly.
Quinine (QUALAQUIN)
MECHANISM OF ACTION
SIDE EFFECTS
nausea.
restlessness.
difficulty hearing or ringing in the ears.
confusion.
Nervousness
Contraindications
Hypersensitivity
G6PD deficiency
Optic neuritis, tinnitus, history of quinine-associated blackwater fever, and
thrombocytopenic purpura
Pregnancy
Nursing considerations
Nursing implications
Be alert for S&S of rising plasma concentration of quinine marked by tinnitus and
hearing impairment, which usually do not occur until concentration is 10 mcg/mL or
more.
Follow the same precautions with quinine as are used with quinidine in patients with
atrial fibrillation; quinine may produce cardiotoxicity in these patients.
DRUG CLASSIFICATION
Mefloquine.
Mechanism of Action:
Membrane-bound mefloquine may inhibit merozoite invasion and interact with proteins
involved with parasite membrane lipid trafficking and nutrient uptake. Mefloquine binds to
haem, forming a complex that may also be toxic to the parasite.
Side effects
nausea
vomiting
fever
diarrhea
loss of appetite
muscle pain
headache
sleepiness
increased sweating
Contraindications
- History of neuropsychiatric disorders including depression and convulsions.
- Hypersensitivity to quinine.
Nursing considerations
- Mefloquine doses in the BNF may differ from those in product literature.
- Travellers should be informed about adverse reactions and, if they occur, that
they should seek medical advice on alternative antimalarials before the next dose
is due.
- Travel to malarious areas should be avoided during pregnancy; if it is
unavoidable, effective prophylaxis must be used but mefloquine should be
avoided as a matter of principle. However, studies of mefloquine use in
pregnancy (including in the first trimester) indicate that it can be considered for
travel to chloroquine-resistant areas.
- Mefloquine is considered to be appropriate for use by people with renal
impairment and does not require dosage reduction.
Drug classification
Pyrimethamine (Daraprim)
Mechanism of Action:
Pyrimethamine inhibits the dihydrofolate reductase of plasmodia and thereby blocks the
biosynthesis of purines and pyrimidines, which are essential for DNA synthesis and cell
multiplication. This leads to failure of nuclear division at the time of schizont formation in
erythrocytes and liver.
Side effects
Contraindications
Use of DARAPRIM is contraindicated in patients with known hypersensitivity to pyrimethamine
or to any component of the formulation. Use of the drug is also contraindicated in patients with
documented megaloblastic anemia due to folate deficiency.
Nursing considerations
Primaque
Mechanism of action
Side effects
Nausea,
vomiting,
dizziness,
stomach upset, and
abdominal cramps
Contraindications
Nursing considerations
Be aware drug may precipitate acute hemolytic anemia in patients with G6PD deficiency,
an inherited error of metabolism carried on the X chromosome
Drug classification
Sulfonamide
Mechanism of action
However, this effect can be reversed by adding the end products of one-carbon transfer reactions, such
as thymidine, purines, methionine, and serine. PABA can also reverse the effects of sulfonamides
Side effects
Lethargy.
Anorexia.
Nausea.
Vomiting.
Dizziness.
Headache.
Photosensitivity (sunburn after exposure to sunlight)
Serious skin rashes. Serious skin rashes include: Steven-Johnson Syndrome,
which causes aching joints and muscles, redness, blistering, and skin peeling.
Contraindications
Sulphanilamide is contraindicated in those known to be hypersensitive to sulfonamides, in nursing
mothers, during pregnancy near term and in infants less than 2 months of age
Nursing considerations
patients should be monitored carefully for adverse effects including delayed hypersensitivity
reactions. Sulfonamide medications increase the risk of crystalluria that can cause kidney
stones or decreased kidney function; therefore, patients should increase their water intake while
taking these medications
Patient teaching
patients should be educated to use sunscreen and protective clothing with sun exposure.
The patient should also report any rash, sore throat, fever, or mouth sores that might occur.
Unusual bleeding or bruising should also be reported to the provider. If patients are receiving
prolonged therapy, they may require platelet count monitoring
Antiprotozoal drugs
Drugs classification
Metronidazole
Mechanism of Action:
.Metronidazole diffuses into the organism, inhibits protein synthesis by interacting with DNA and
causing a loss of helical DNA structure and strand breakage. Therefore, it causes cell death in susceptible
organisms.
The mechanism of action of metronidazole occurs through a four-step process. Step one is the
entry into the organism by diffusion across the cell membranes of anaerobic and aerobic
pathogens. However, antimicrobial effects are limited to anaerobes. Step two involves reductive
activation by intracellular transport proteins by altering the chemical structure of pyruvate-
ferredoxin oxidoreductase. The reduction of metronidazole creates a concentration gradient in
the cell that drives uptake of more drug and promotes free radical formation that is
cytotoxic. Step three, interactions with intracellular targets, is achieved by cytotoxic particles
interacting with host cell DNA resulting in DNA strand breakage and fatal destabilization of the
DNA helix. Step four is the breakdown of cytotoxic products. Metronidazole is also cytotoxic to
facultatively anaerobic bacteria like Helicobacter pylori and Gardnerella vaginalis, but the
mechanism of action to these pathogens is not well understood.
Side Effects:
Dizziness, headache, stomach upset, nausea, vomiting, loss of
appetite, diarrhea, constipation, or metallic taste in your mouth may occur
Contraindications
Pregnancy, 1st trimester (controversial)
Use of disulfiram within past 2 weeks; use of alcohol during therapy or within 3 days of discontinuing
therapy
Nursing considerations
Take full course of drug therapy; take the drug with food if GI upset occurs.
Do not drink alcohol (beverages or preparations containing alcohol, cough syrups); severe reactions may
occur.
Your urine may be a darker color than usual; this is expected.
Refrain from sexual intercourse during treatment for trichomoniasis, unless partner wears a condom.
Apply the topical preparation by cleansing the area and then rubbing a thin film into the affected area.
Avoid contact with the eyes. Cosmetics may be applied to the area after application.
You may experience these side effects: Dry mouth with strange metallic taste (frequent mouth care,
sucking sugarless candies may help); nausea, vomiting, diarrhea (eat frequent small meals).
Drug classification
Paromomycin
Mechanism of action
Paromomycin inhibits protein synthesis by binding to 16S ribosomal RNA. Bacterial proteins are
synthesized by ribosomal RNA complexes which are composed of 2 subunits, a large subunit (50s) and
small (30s) subunit, which forms a 70s ribosomal subunit. tRNA binds to the top of this ribosomal
structure. Paramomycin binds to the A site, which causes defective polypeptide chains to be produced.
Continuous production of defective proteins eventually leads to bacterial death.
Side effects
Contraindications
Paromomycin sulfate (paromomycin sulfate (paromomycin sulfate capsules) capsules) is
contraindicated in individuals with a history of previous hypersensitivity reactions to it. It is also
contraindicated in intestinal obstruction.
Nursing considerations
Patient/Client-Related Instruction
Drug classification
Atovaquone(mepron)
Mechanism of Action
Atovaquone possesses a novel mode of action against P. falciparum through inhibition of the electron
transport system at the level of cytochrome bc1 complex. Atovaquone also causes collapse of the
parasite mitochondrial membrane potential in P. falciparum. The mechanism of action against P.
carinii is unknown. The synergistic activity between proguanil and atovaquone appears to be related to
proguanil per se, and metabolism to cycloguanil is not required.
Side effects
nausea.
vomiting.
diarrhea.
headache.
dizziness.
anxiety.
difficulty falling asleep or staying asleep.
Contraindications
Contraindicated in patients who develop or have a history of hypersensitivity reactions (e.g.,
angioedema, bronchospasm, throat tightness, urticaria) to atovaquone or any of the
components of atovaquone oral suspension.
Nursing consideration
Assess pulmonary function by measuring lung volumes, breath sounds, respiratory rate,
and other symptoms (cough, dyspnea, shortness of breath).
Report changes in pulmonary function to help document the effects of drug therapy in
treating PCP infections.
Patient/Client-Related Instruction
Remind patient to take this drug as directed for the full course of treatment even if feeling
better.
Instruct patient and family/caregivers to report other troublesome side effects such as
severe or prolonged headache, sleep loss, skin rash, fever, or GI problems (diarrhea,
nausea, vomiting).
Drug classification
Pentamidine
Mechanism of action
Contraindications
Congenital QT syndrome
Electrolyte abnormalities, uncorrected
Nursing considerations
Assess heart rate, ECG, and heart sounds, especially during exercise Report any rhythm
disturbances or symptoms of cardiac dysfunction, including palpitations, chest discomfort,
shortness of breath, fainting, and fatigue/weakness.
Monitor signs of pancreatitis, including upper abdominal pain (especially after eating),
indigestion, weight loss, oily stools. Report these signs to the physician immediately.
Assess blood pressure (BP) periodically and compare to normal Report low BP (hypotension)
Albendazole
Mechanism of action
The principal mode of action for albendazole is by its inhibitory effect on tubulin polymerization
which results in the loss of cytoplasmic microtubules in the intestines of nematodes worms,
ultimately causing energy depletion and death of the organism
Contraindications
Adverse effects
Abdominal pain
Nausea
Vomiting
Headache
Dizziness
Fever
Nursing considerations
Assess for the mentioned cautions and contraindications (e.g. known allergies,
hepatorenal dysfunction, pregnancy and lactation, etc.) to prevent any untoward
complications.
Perform a thorough physical assessment (other medications taken, reflexes
and muscle strength, skin color, temperature, texture, etc.) to establish baseline data
before drug therapy begins, to determine effectiveness of therapy, and to evaluate for
occurrence of any adverse effects associated with drug therapy.
Assess the patient’s liver function, including liver function tests to determine
appropriateness of therapy and to monitor for toxicity.
Obtain a culture of stool for ova and parasites to determine the infecting worm and
establish appropriate treatment.
Assess the abdomen to evaluate for any changes from baseline related to the infection,
identify possible adverse effects, and monitor for improvement.
Drug classification
Pyrantel pamoate
Mechanism of action
Side effects
Contraindications
Hepatic disease
Pyrantel should be used with caution in patients with hepatic disease.
Phenylketonuria
Pyrantel chewable tablets contain phenylalanine; use with caution in patients with phenylketonuria.
Pregnancy
Pyrantel is poorly absorbed from the GI tract. There are no well controlled studies of pyrantel use in
pregnant women. Use pyrantel with caution during pregnancy. Some experts suggest that single-
dose pyrantel therapy may be given to pregnant women. Pregnant women should not take pyrantel
unless directed by a doctor.
Breast-feeding
There are no data regarding the presence of pyrantel in breast milk. Pyrantel is poorly absorbed
from the GI tract; therefore, excretion into breast milk may be minimal. Some experts suggest single-
dose pyrantel therapy may be given to breast-feeding women. Breast-feeding infant exposure may
be minimized if the drug is taken just before the longest sleep interval for the infant
Nursing considerations
Monitor baseline and periodic AST/ALT in individuals with known liver dysfunction.
Do not drive or engage in other potentially hazardous activities until response to drug is
known.
Do not breast feed while taking this drug without consulting physician.
Drug classification
Biltricide(praziquantel)
Mechanism of action
The drug's mode of action is not exactly known at present, but experimental evidence
indicates praziquantel increases the permeability of the membranes of schistosome cells
towards calcium ions. The drug thereby induces contraction of the parasites' muscle, resulting
in paralysis in the contracted state. The dying parasites are dislodged from their site of action
in the host organism and may enter systemic circulation or may be destroyed by host immune
reaction (phagocytosis).
Side effects
Nursing considerations
Do not drive or operate other hazardous machinery on day of treatment or the following
day because of potential drug-induced dizziness and drowsiness.
Usually, all schistosomal worms are dead 7 d following treatment.
Contact physician if you develop a sustained headache or high fever.
Do not breast feed while taking this drug without consulting physician
Drug classification
Ivermectin
Mechanism of action
Ivermectin and its related drugs act by interfering with the nerve and muscle functions
of helminths and insects. The drug binds to glutamate-gated chloride channels common to
invertebrate nerve and muscle cells. The binding pushes the channels open, which increases the
flow of chloride ions and hyper-polarizes the cell membranes, paralyzing and killing the invertebrate.
Ivermectin is safe for mammals (at the normal therapeutic doses used to cure parasite infections)
because mammalian glutamate-gated chloride channels only occur in the brain and spinal cord: the
causative avermectins usually do not cross the blood–brain barrier, and are unlikely to bind to other
mammalian ligand-gated channels. \
Side effects