Chloroquine
Pronunciation: (KLOR-oh-kwin)Class: 4-aminoquinoline compound, Amebicide
Trade Names:
Aralen Phosphate
- Tablets 500 mg chloroquine phosphate (equivalent to 300 mg base)
Pharmacology
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Inhibits parasite growth, possibly by concentrating within parasite acid vesicles, raising pH.
Pharmacokinetics
Absorption
Rapidly and almost completely absorbed from the GI tract.
Distribution
About 55% bound to nondiffusable plasma constituents. Distributed considerably into tissues (ie, liver, spleen, kidney, lung) and to a lesser extent into brain and spinal cord.
Metabolism
The main metabolite is desethylchloroquine.
Elimination
Slowly excreted, but increased by acidification of the urine. A small amount is excreted in the feces. About 25% of the dose is excreted in urine as desethylchloroquine. More than 50% of urinary drug product is unchanged chloroquine.
Indications and Usage
Prophylaxis and treatment of acute attacks of malaria caused by Plasmodium vivax , Plasmodium malariae , Plasmodium ovale , and susceptible strains of Plasmodium falciparum ; extraintestinal amebiasis.
Unlabeled Uses
Treatment of rheumatoid arthritis, systemic and discoid lupus erythematosus, porphyria cutanea tarda, scleroderma, pemphigus, lichen planus, polymyositis, and sarcoidosis.
Contraindications
Retinal or visual field changes.
Dosage and Administration
Doses are listed in base equivalents.
Acute MalariaAdults
PO Initial dose is 600 mg, then 300 mg 6 h later and 300 mg every day for 2 days.
ChildrenPO Initial dose is 10 mg/kg, then 5 mg/kg 6 h later and 5 mg/kg every day for 2 days.
Malaria SuppressionAdults
PO 300 mg base.
Children5 mg/kg/dose (max 300 mg base) weekly. Begin 1 to 2 wk prior to exposure and continue for 4 wk after leaving endemic area. If suppressive therapy is not begun prior to exposure, double initial loading dose and give in 2 divided doses 6 h apart.
Extraintestinal AmebiasisAdults
PO 600 mg base/day for 2 days, then 300 mg base/day for 2 to 3 wk.
General Advice
- Administer with food or milk.
- If taken once weekly, take on same day of week.
Storage/Stability
Store in airtight, light-resistant container at room temperature.
Drug Interactions
CimetidineMay increase chloroquine serum concentration.
Kaolin aluminum or magnesium trisilicate antacidsMay decrease GI absorption of chloroquine.
Rabies vaccineCoadministration of intradermally administered rabies vaccine and chloroquine may result in diminished antibody response to vaccine. In this situation CDC recommends administering rabies vaccine IM.
Laboratory Test Interactions
None well documented.
Adverse Reactions
Cardiovascular
Hypotension; ECG changes.
CNS
Headache; neuropathy; seizures; psychotic episodes.
Dermatologic
Pruritus; pigment changes; skin eruptions.
EENT
Visual disturbances; retinal damage and deafness with prolonged high-dose use; tinnitus.
GI
Anorexia; nausea; vomiting; diarrhea; abdominal cramps.
Hematologic
Agranulocytosis; blood dyscrasias; aplastic anemia.
Hepatic
Hepatitis.
Miscellaneous
Muscle weakness.
Precautions
MonitorNeuromuscular examPerform periodic neuromuscular examinations and notify patient if knee and ankle reflexes are weak. Adverse reactionsIf sore throat, fever, weakness, fatigue, or unusual bleeding or bruising occurs, notify health care provider. |
Pregnancy
Category D .
Lactation
Excreted in breast milk.
Children
Especially sensitive to adverse reactions; do not exceed recommended dose.
Special Risk Patients
Monitor patients with hepatic disease or alcoholism, or taking other hepatotoxic medications for evidence of worsening liver function such as bleeding.
G-6-PD deficiency
May induce hemolysis in presence of infection or stressful condition.
Muscular weakness
May need to discontinue therapy if muscle weakness occurs.
Psoriasis or porphyria
May be exacerbated.
Retinopathy
Irreversible retinal damage has occurred.
Overdosage
Symptoms
Headache, drowsiness, visual disturbances, CV collapse, seizures, respiratory and cardiac arrest, death.
Patient Information
- Remind patient to take medication with food to minimize GI irritation.
- Stress importance of compliance with full course of therapy. If used for suppression, drug must be taken at least 1 wk before entering and for 4 wk after leaving endemic area.
- Caution patient to drink alcoholic beverages sparingly because of increased GI irritation and higher risk of liver damage.
- Stress importance of eye examinations every 3 to 6 mo during prolonged daily therapy.
- Inform patient that drug may cause rusty or brown discoloration of urine.
- Advise use of dark glasses in bright light to reduce risk of ocular damage.
- Instruct patient to report these symptoms to health care provider: blurring or change in vision, buzzing or difficulty hearing, muscle weakness, rash, vomiting or stomach pain, difficulty breathing or swallowing.
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More Chloroquine resources
chloroquine Oral, Intramuscular - Includes detailed dosage instructions.
Compare Chloroquine with other medications for the treatment of:
Malaria Prevention, Malaria, Sarcoidosis, Amebiasis
