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Chloroquine information from DrugsUpdate  

See Available Brands of Chloroquine in India

P - Caution when used during pregnancy
L - Caution when used during lactation

Chloroquine is a 4-aminoquinoline drug used in the treatment or prevention of malaria.

Pharmacodynamics

Pharmacokinetics

Chloroquine is used for malarial prophylaxis (as a suppressive) and in managing acute attacks of malaria. It is highly active against erythrocytic forms of P. vivax, P. malariae and P. falciparum. It influences Hb digestion by increasing intravesicular pH in malaria parasite cells and interferes with the nucleoprotein synthesis of the patient. It is also effective in extra intestinal amoebiasis. In RA chloroquine and more effectively hydroxychloroquine have a disease-modifying effect.


Absorption
Rapid and complete (oral); rapid (IM/SC).

Distribution
Widely distributed; high concentrations in kidneys, liver, lungs and spleen; crosses the placenta; enters breast milk.

Metabolism
Extensively hepatic; converted to monodesethylchloroquine.

Excretion
Urine (as unchanged drug and metabolite).

Chloroquine Indications / Chloroquine Uses

Information Not Available

Chloroquine Adverse Reactions / Chloroquine Side Effects

Retinopathy, hair loss, photosensitivity, tinnitus, myopathy (long-term therapy). Psychosis, seizures, leucopenia and rarely aplastic anaemia, hepatitis, GI upsets, dizziness, hypokalaemia, headache, pruritus, urticaria, difficulty in visual accommodation. Potentially Fatal: Cardiac and respiratory arrest, CV collapse, convulsions, coma.

Precautions

Effects/Laboratory Tests
Complete blood cell counts should be made periodically if patients are given prolonged therapy. If any severe blood disorder appears which is not attributable to the disease under treatment, discontinuance of the drug should be considered.
The drug should be administered with caution to patients having G-6-PD (glucose-6 phosphate dehydrogenase) deficiency.

Auditory Effects
In patients with preexisting auditory damage, Chloroquine should be administered with caution. In case of any defects in hearing, Chloroquine should be immediately discontinued, and the patient closely observed.

Hepatic Effects
Since this drug is known to concentrate in the liver, it should be used with caution in patients with hepatic disease or alcoholism or in conjunction with known hepatotoxic drugs.

Central Nervous System Effects
Patients with a history of epilepsy should be advised about the risk of Chloroquine provoking seizures.

Drug Interactions
Antacids and kaolin:Antacids and kaolin can reduce the absorption of Chloroquine; an interval of at least 4 hours between intake of these agents and Chloroquine should be observed.

Cimetidine
Cimetidine can inhibit the metabolism of Chloroquine, increasing its plasma level. Concomitant use of cimetidine should be avoided.


Ampicillin
In a study of healthy volunteers, Chloroquine significantly reduced the bioavailability of ampicillin. An interval of at least two hours between intake of this agent and Chloroquine should be observed.

Cyclosporine
After introduction of Chloroquine (oral form), a sudden increase in serum cyclosporine level has been reported. Therefore, close monitoring of serum cyclosporine level is recommended and, if necessary, Chloroquine should be discontinued.

Overdosage
Symptoms include headache, drowsiness, visual disturbances, nausea and vomiting, CV collapse, shock and convulsions followed by sudden and early respiratory and cardiac arrest. ECG may reveal atrial standstill, nodal rhythm, prolonged intraventricular conduction time and progressive bradycardia leading to ventricular fibrillation and/or arrest. Treatment is symptomatic and should be prompt with immediate evacuation of the stomach by emesis or gastric lavage. Finely powdered, activated charcoal may be used within 30 min after ingestion of the antimalarial to reduce intestinal absorption of the drug. To be effective, the dose of activated charcoal should be at least five times the estimated dose of chloroquine ingested.

Special Precautions

Psoriasis, diseases of the haematopoietic or CNS systems, myasthenia gravis, hepatic or renal impairment, G6PD deficiency, epilepsy, childn. Pregnancy and lactation. Slow infusion is used upon IV admin to prevent cardiotoxicity.

Other Drug Interactions

Concomitant therapy with phenylbutazone predisposes to dermatitis, antagonises effect of neostigmine and pyridostigmine, reduces bioavailability of ampicillin. Cimetidine inhibits metabolism of chloroquine raising plasma levels.


Potentially Fatal: Increased risks of inducing ventricular arrhythmias with halofantrine or other arrhythmogenic drugs eg, amiodarone. Increased risk of convulsions with mefloquine. Antacids reduce absorption of chloroquine hence admin should be separated by 4 hrs. Rarely Stevens-Johnson syndrome, when administered with pyrimethamine/sulphadoxine. Increased toxicity with quinacrine.

Other Interactions

Information Not Available

Dosage

Oral Acute malaria
Adult: As base: Initially, 600 mg followed by 300 mg 6-8 hours later on day 1. On days 2 and 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 hours. Single doses of 5 mg base/kg on days 2 and 3.

Elderly:Oral Prophylaxis of malaria
Adult: As base: 300 mg once weekly, starting 1 week before exposure, continuing throughout on a weekly basis and for at least 4 wk after exposure.
Child: 5 mg/kg weekly.

Oral Discoid and 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.

Elderly:Oral Hepatic amoebiasis
Adult: As base: 600 mg daily for 2 days then 300 mg daily for 2 or 3 wk given with emetine or dehydroemetine.
Child: 6 mg/kg daily. Max dose: 300 mg daily.

Oral Rheumatoid arthritis
Adult: As base: 150 mg daily. Max: 2.5 mg/kg daily. Discontinue treatment if there is no improvement after 6 month.
Child: Up to 3 mg/kg/day. Discontinue treatment if there is no improvement after 6 mth. Renal impairment: May need to reduce dose in prolonged treatment.

Intravenous Severe and complicated malaria
Adult: As base: 25 mg/kg given in several infusions over 30-32 hours at a slow rate. May start on oral therapy once patient is able to tolerate oral doses.

Food(before/after)

Should be taken with food.

List of Contraindications

Chloroquine and Pregnancy

Caution when used during pregnancy.


Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Chloroquine and Lactation

Caution when used during lactation

Chloroquine and Children

Hypersensitivity, known or suspected resistant P. falciparum infection, porphyria, retinal damage, concurrent hepatotoxic drugs.

Chloroquine and Geriatic

Information Not Available

Chloroquine and Other Contraindications

Information Not Available

Storage

Intravenous
Store at 15-30°C.

Oral
Store at 15-30°C.

Lab interference

Intravenous
Store at 15-30°C.

Oral
Store at 15-30°C.

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