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May 1980

Antimalarial Agents: Chloroquine, Hydroxychloroquine, and Quinacrine

Author Affiliations

From the Dermatology Service, San Francisco Veterans Administration Center (Dr Tanenbaum), and the Department of Dermatology, University of California, San Francisco (Drs Tanenbaum and Tuffanelli).

Arch Dermatol. 1980;116(5):587-591. doi:10.1001/archderm.1980.01640290097026

Chloroquine phosphate and hydroxychloroquine sulfate are substituted 4-amino quinoline compounds that differ only by a hydroxy group. Quinacrine hydrochloride also has the 4-amino quinoline radical but has, in addition, a benzene ring; it is classified as an acridine compound. The 4-amino quinoline radical is present in all antimalarial compounds shown to be effective in the treatment of lupus erythematosus (LE) (Figure).1

HISTORY  Quinacrine was introduced for malaria therapy in 1930. Its superiority over quinine was established during World War II, when it became the official drug for the treatment of malaria. The toxicity of quinacrine and its inability either to cure malaria or to act as an effective prophylactic, however, spurred continued research for better drugs. A large series of 4-amino quinolines were investigated. Of these, chloroquine proved to be the most promising and was released for field trial.2 By the end of World War II, it had

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