Chloroquine
- Atc Codes:P01BA01
- CAS Codes:54-05-7#50-63-5
- PHARMGKB ID:54-05-7#50-63-5
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Resochin; Belgium: Nivaquine; Bulgaria: Resochin; Cyprus: Chloroquine; Czech Republic: Delagil; Denmark: Malarex; Finland: Heliopar; France: Nivaquine; Germany: Chloroquin, Resochin, Resochina; Hungary: Delagil; Italy: Cloroc Fos, Clorochina; Luxembourg: Nivaquine; Malta: Avlocor; Netherlands: Nivaquine; Poland: Arechin; Portugal: Cloroquina, Resochina; Slovakia: Delagil; Spain: Resochin; Sweden: Klorokinfosfat; UK: Avloclor, Nivaquine.
North America
Canada: Chloroquine; USA: Aralen, Chloroquine.
Latin America
Argentina: Nivaquine; Brazil: Diclokin, Quinacris; Mexico: Aralen.
Drug combinations
Chloroquine and Proguanil
Chemistry
Chloroquine: C~18~H~26~ClN~3~. Mw: 319.87. (1) 1,4-Pentanediamine, N^4^-(7-chloro-4-quinolinyl)-N^1^,N^1^-diethyl-; (2) 7-Chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]quinoline. CAS-54-05-7.
Chloroquine Phosphate: C~18~H~26~ClN~3~ 2H~3~PO~4~. Mw: 515.86. 7-Chloro-4-[[4-(diethylamino)-1-methylbutyl]amino]quinoline phosphate (1:2). CAS-50-63-5.
Pharmacologic Category
Antiprotozoals; Antimalarials. (ATC-Code: P01BA01).
Mechanism of action
Binds to and inhibits DNA and RNA polymerase. Interferes with metabolism and hemoglobin utilization by parasites. Inhibits prostaglandin effects. May involve aggregates of ferriprotoporphyrin IX acting as chloroquine receptors causing membrane damage. May also interfere with nucleoprotein synthesis. Active against asexual erythrocytic forms of most strains of Plasmodium malariae, P. ovale, P. vivax, and many strains of P. falciparum. Not active against preerythrocytic or exoerythrocytic forms of plasmodia. Gametocytocidal for P. malariae and P. vivax (no direct activity against gametocytes of P. falciparum). Chloroquine-resistant P. falciparum are also resistant to hydroxychloroquine and may be cross-resistant to pyrimethamine or quinine. Active in vitro against the trophozoite form of Entamoeba histolytica (acts as a tissue amebicide). Has anti-inflammatory activity (mechanism(s) of action in treatment of rheumatoid arthritis and lupus erythematosus not determined).
Therapeutic use
Suppression or chemoprophylaxis of malaria. Uncomplicated or mild-to-moderate malaria. Extraintestinal amebiasis.
Pregnancy and lactiation implications
There are no adequate studies on use of chloroquine during pregnancy. Chloroquine prophylaxis may be considered in areas of chloroquine-sensitive P. falciparum malaria. Use not recommended during lactation.
Unlabeled use
Rheumatoid arthritis. Discoid lupus erythematosus. Porphyria cutanea tarda. Polymorphous light eruptions. Sarcoidosis.
Contraindications
Hypersensitivity to chloroquine or any component. Retinal or visual field changes. Psoriasis. Avoid use in pregnancy except in the suppression or treatment of malaria when benefit outweighs potential risk to the fetus.
Warnings and precautions
Chloroquine has been associated with ECG changes, AV block, and cardiomyopathy (rare). Aminoquinolones have been associated with rare hematologic reactions including agranulocytosis, aplastic anemia, and thrombocytopenia. Myopathy, neuromyopathy, and progressive weakness reported with aminoquinolones (chloroquine). Dose-related (may be reversible) retinopathy, blurred vision or keratopathy have occurred with chloroquine. Use with caution in pre-existing auditory damage. Use with caution in known G6PD deficiency. Use with caution in hepatic impairment, alcoholism, or concurrent therapy with hepatotoxic agents. Use with caution in porphyria, and in psoriasis (may exacerbate symptoms). Use with caution in history of seizures.