Studies on the Pharmacology of Chloroquine

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Abstract
Introduction Chloroquine (7-chloro-4- (4-diethylamino1-methylbutylamino) quinoline (Fig 1) was originally developed as an antimalarial agent. In recent years it has been found to be beneficial in a variety of diseases, including rheumatoid arthritis, discoid and systemic lupus erythematosus. When used as a malarial suppressive, 500 mg of chloroquine salt are given once a week. In the treatment of diseases other than malaria, chloroquine is administered in a much larger dosage and more frequently, usually 250 to 750 mg daily.1 The occurrence of a characteristic retinopathy following the long-term daily ad- ministration of chloroquine has now been well documented.2The fact that the retinal lesion usually develops after one or more years of drug ingestion, plus the remarkably large accumulation of chloroquine in body tissues and organs,3-5suggests that the retinopathy may be due to high chloroquine levels in the ocular tissues. The present report concerns the finding of