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.1The occurrence of a characteristic retinopathy following the long-term daily ad- ministration of chloroquine has now been well documented.2 The 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,3-5 suggests that the retinopathy may be due to high chloroquine levels in the ocular tissues. The present report concerns the finding of
RUBIN M, BERNSTEIN HN, ZVAIFLER NJ. Studies on the Pharmacology of Chloroquine: Recommendations for the Treatment of Chloroquine Retinopathy. Arch Ophthalmol. 1963;70(4):474–481. doi:10.1001/archopht.1963.00960050476009
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