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Journal of Pharmacology And Experimental Therapeutics, Vol. 187, Issue 1, 138-151, 1973
Copyright © 1973 by American Society for Pharmacology and Experimental Therapeutics

STUDIES OF THE METABOLISM OF DAPSONE IN MAN AND EXPERIMENTAL ANIMALS: FORMATION OF N-HYDROXY METABOLITES

Z. H. Israili 1, S. A. Cucinell 1, J. Vaught 1, E. Davis 1, J. M. Lesser 1, and P. G. Dayton 1

1 Clinical Pharmacology Program and Department of Medicine, Emory University School of Medicine, Atlanta, Georgia

As an extension of our in vitro studies [in which we showed that dapsone (DDS) is N-oxidized by rat liver microsomes to its monohydroxylamine and that this metabolite is responsible for methemoglobinemia] we investigated the metabolism of DDS and diformyl dapsone in man and DDS in rats and guinea pigs. In man given DDS-14C or diformyl dapsone-14C, urine represented the major route of elimination of radioactivity. Significant amounts of N-oxidations metabolites were found in urine. One of the primary urinary N-oxidation metabolites, the monohydroxylamine of dapsone, was isolated and characterized as azoxy-DDS. A new metabolite—the monohydroxylamine of 4-acetylamino-4' aminodiphenylsulfone—was also identified. N-oxidation metabolites accounted for a small fraction of the dose of DDS-14C in animal urine and and liver: the amount in bile was higher. A number of metabolites and derivatives of DDS were synthesized and tested for their ability to produce methemoglobin.

Submitted on December 13, 1972
Accepted on June 5, 1973




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