Composition
Each tablet contains: Chloroquine phosphate 250mg Each 5ml (teaspoonful) of syrup contains: Chloroquine phosphate 80mg

Description

 Chloroquine contains chloroquine phosphate, a 4-aminoquinoline. It is a rapidly acting schizonticide, well tolerated and safe. It is indicated for the treatment of malarial infection caused by Plasmodium species.

Pharmacology

Mircobiology: Chloroquine has been found to be highly active against the erythrocytic forms of Plasmodium vivax and malariae and most strains of Plasmodium falciparum. The precise mechanism of action of the drug is unknown. While the drug can inhibit certain enzymes, its effect is believed to result from its interaction with DNA. It appears that it acts against the blood schizonts by influencing haemoglobin digestion by the malarial parasites. Chloroquine also possesses amoebicidal activity comparable to that of emetine.

Pharmacokinetics (Absorption): Rapid peak blood levels are achieved in 1 to 2 hours

Distribution: It is widely distributed throughout the body and present in high concentrations in the liver, kidneys, lungs and crosses the placenta and appears in breast milk

Protein binding: About 50% to 65%

Excretion: Approximately 70% of a dose is excreted unchanged in the urine, and 10% in faeces. Acidification of the urine increases elimination of the drug. Small amounts of the drug may be present in the urine months following discontinuation of therapy.

Indications

Chloroquine is the drug of choice in the treatment of acute attacks due to P. vivax, P. ovale, P. malariae and susceptible strains of P. falciparum.

Dosage and Administration

Adult: An initial loading dose of four (1000mg) Choroquine tablets. This is followed by another four (1000mg) tablets on the second day and two tablets (500mg) on the third day.

Children: The initial dose is 17mg/kg (or calculated on base 10mg/kg), but a single dose should not exceed 1000mg. Treatment should continue the following day with another dose of 17mg/kg (or calculated on base 10mg/kg; on the third day 8.5mg/kg (or calculated on base 5mg/kg) should be administered.

Contraindications

Known or suspected chloroquine resistance in Plasmodium falciparum, porphyria, retinal damage, concurrent therapy with hepatotoxic drugs and previous hypersensitivity to chloroquine.

Warning and Precautions Some strains of P. falciparium are resistant to 4-aminoquinoline compounds, so treatment with quinine or other specific treatment should be considered in such cases. Irreversible retinal damage has been observed in long term/high dosage treatment. So periodic ophthalmological examination should be contemplated. Muscular weakness may occur with chloroquine phosphate treatment. It may precipitate a severe attack of psoriasis. In patients with porphyria, condition may be exacerbated, in such patients the drug is to be withdrawn or avoided.

Side Effects

Anorexia, nausea, vomiting, diarrhoea, abdominal cramps, hypotension and ECG changes, mild headache, psychic stimulation, have been reported with chloroquine phosphate. Rarely nerve type deafness, tinnitis and reduced hearing may occur in few patients. Irreversible retinal damage, visual disturbance, scotomatous vision with field defects may also occur at times. Other side effects such as agranulocytosis, pruritis, neuropathy, blood dyscrasia, mucosal pigmentary changes and pleomorphic skin eruptions have been reported on prolonged therapy.

Presentation

Choloquine is available as Tablets (10’s and 1000’s) and Syrup (60ml).