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Dapsone Acetylation and the Treatment of Leprosy

Abstract

DAPSONE (4,4′-diaminodiphenyl sulphone, DDS) continues to be the standard drug for the treatment of leprosy. Recent studies1 have shown that DDS is converted in man to monoacetyldapsone (MADDS) in a polymorphic fashion by the same enzyme system that acetylates isoniazid and sulphamethazine. Unlike acetylisoniazid and acetylsulphamethazine, however, MADDS is rapidly deacetylated in man. Consequently, constant plasma ratios of acetylated to parent drug are found almost immediately after dosage with DDS, and significantly higher ratios are found in rapid acetylators of isoniazid or sulphamethazine than in slow acetylators. The half-life of DDS in the body, unlike that of isoniazid, seems to be unrelated to the speed at which it is acetylated.

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ELLARD, G., GAMMON, P., HELMY, H. et al. Dapsone Acetylation and the Treatment of Leprosy. Nature 239, 159–160 (1972). https://doi.org/10.1038/239159a0

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