Brands, Medical Use, Clinical Data
Drug Category
- Antirheumatic Agents
- Antimalarials
- Amebicides
Dosage Forms
Brands / Synonyms
3377 RP opalate; Amokin; Aralen; Aralen HCl; Arechin; Arthrochin; Artrichin; Avlochlor; Avloclor; Bemaco; Bemaphate; Bemasulph; Benaquin; Bipiquin; Capquin; Chemochin; Chingamin; Chloraquine; Chlorochin; Chlorochine; Chloroquina; Chloroquine (VAN); Chloroquine Phosphate; Chloroquinium; Chlorquin; Cidanchin; Clorochina; Cocartrit; Delagil; Dichinalex; Elestol; Gontochin; Heliopar; Hydroxychloroquine Sulfate; Imagon; Iroquine; Klorokin; Lapaquin; Malaquin; Malaren; Malarex; Mesylith; Neochin; Nivachine; Nivaquine; Nivaquine B; Nivaquine [as sulfate]; Pfizerquine; Plaquenil; Quinachlor; Quinagamin; Quinagamine; Quinercyl; Quingamine; Quinilon; Quinoscan; Resochen; Resochin; Resoquina; Resoquine; Reumachlor; Reumaquin; Roquine; Sanoquin; Silbesan; Siragan; Solprina; Sopaquin; Tanakan; Tresochin; Trochin
Indications
For the suppressive treatment and for acute attacks of malaria due to P. vivax, P.malariae, P. ovale, and susceptible strains of P. falciparum, Second-line agent in treatment of Rheumatoid Arthritis
Pharmacology
Chloroquine is the prototype anti malarial drug, most widely used to treat all types of malaria except for disease caused by chloroquine resistant Plasmodium falciparum. It is highly effective against erythrocytic forms of Plasmodium vivax, Plasmodium ovale and Plasmodium malariae, sensitive strains of Plasmodium falciparum and gametocytes of Plasmodium vivax. Being alkaline, the drug reaches high concentration within the food vacuoles of the parasite and raises its pH. It is found to induce rapid clumping of the pigment. Chloroquine inhibits the parasitic enzyme heme polymerase that converts the toxic heme into non-toxic hemazoin, thereby resulting in the accumulation of toxic heme within the parasite. It may also interfere with the biosynthesis of nucleic acids.
Mechanism of Action
The mechanism of plasmodicidal action of chloroquine is not completely certain. Like other quinoline derivatives, it is thought to inhibit heme polymerase activity. This results in accumulation of free heme, which is toxic to the parasites.
Absorption
Completely absorbed from gastrointestinal tract
Toxicity
Not Available
Biotrnasformation / Drug Metabolism
Hepatic (partially)
Contraindications
Use of this drug is contraindicated in the presence of retinal or visual field changes either attributable to 4-aminoquinoline compounds or to any other etiology, and in patients with known hypersensitivity to 4-aminoquinoline compounds. However, in the treatment of acute attacks of malaria caused by susceptible strains of plasmodia, the physician may elect to use this drug after carefully weighing the possible benefits and risks to the patient.
Drug Interactions
Antacids and kaolin: Antacids and kaolin can reduce 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.
Cyclosporin: After introduction of chloroquine (oral form), a sudden increase in serum cyclosporin level has been reported. Therefore, close monitoring of serum cyclosporin level is recommended and, if necessary, chloroquine should be discontinued.
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