Treatment of uncomplicated malaria due to susceptible strains of P. falciparum, P. malariae, P. ovale, and P. vivax. Prophylaxis of malaria in geographic areas without resistance to chloroquine.
4-aminoquinoline Derivatives; Antimalarial/ Antirheumatoid/Amoebicide
Chloroquine Phosphate is a 4-aminoquinoline antimalarial and amoebicidal agent used for the suppression and clinical cure of malaria due to susceptible strains of Plasmodium falciparum, P. ovale, P. vivax and P. malariae. It is a rapidly acting blood schizontocide with some gametocytocidal activity. Its mechanism of action against blood schizonts remain unclear but it may act by influencing haemoglobin digestion by raising intravesicular pH in malaria parasite cells. It also inferferes with synthesis of nucleoproteins by the parasite. Chloroquine is rapidly and almost completely absorbed from the gastro-intestinal tract when given by mouth. Absorption is also rapid following intramuscular or subcutaneous administration. About 55% of chloroquine in the circulation is bound to plasma proteins.
ORAL Acute malaria: Adult: As base: Initially, 600 mg followed by 300 mg 6-8 hr later on day 1. On days 2&3, single doses of 300 mg/day. Child: Initially. 10 mg base/ kg (max 600 mg base) followed by 5 mg base/kg (max 300 mg base) after 6 hrs. Single doses of 5 mg base/ kg on days2&3. Prophylaxis of malaria: Adult: As base: 300 mg once wkly, starting 1 wk before exposure, continuing throughout on a wkly basis & for at least 4 wk after exposure. Child: 5 mg/kg weekly. Discoid & systemic lupus erythematosus: Adult: As base: Initially, 150 mg once daily, reduce gradually after maximal response. Max dose: 2.5 mg/kg daily. Child: 3 mg/kg daily. INTRAVENOUS Severe & complicated malaria: Adult: As base: 25 mg/kg given in several infusions over 30-32 hr at a slow rate. May start on oral therapy once patient is able to tolerate oral doses.
Chloroquine exhibits interaction with the drugs like neostigmine, pyridostigmine, antacids, kaolin, cimetidine, ranitidine, quinine, mefloquine, amodiaquine, artemisinin, metronidazole, ampicillin.
Hypersensitivity, known or suspected resistant P. falcipansm infection, porphyria, retinal damage, concurrent hepatotoxic drugs. Psoriasis, diseases of the haematopoietic or CNS systems, myasthenia gravis, hepatic or renal impairment, G6PD deficiency, epilepsy, childn. Pregnancy & lactation. Slow infusion is used upon IV admin to prevent cardiotoxicity.
Retinopathy, hair loss, photosensitivity, tinnitus, myopathy (long-term therapy). Psychosis. seizures, leucopenia & rarely aplastic anaemia, hepatitis, GI upsets, dizziness, hypokalaemia, headache, pruritus, urticaria, difficulty in visual accommodation. Cardiac & resp arrest, CV collapse, convulsions, coma.
There is no evidence that chloroquine is harmful in prophylactic doses during pregnancy. Because of the susceptibility of pregnant women to falciparum malaria, it should be used at the recommended dosage for both prophylaxis and treatment wherever chloroquine-sensitive malaria is prevalent. The maximum daily dose of the drug that the infant can receive from breastfeeding was about 0.7% of the maternal start dose of the drug in malaria chemotherapy. It is, therefore, suggested that it is safe for mothers to breastfeed their infants when undergoing treatment for malaria with chloroquine.
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
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