METABOLISM OF CLOFAZIMINE IN LEPROSY PATIENTS

  • 1 January 1981
    • journal article
    • research article
    • Vol. 9  (6) , 521-524
Abstract
Two metabolites of clofazimine (B663; Lamprene; 3-(p-chloroanilino)-10-(p-chlorophenyl)-2,10-dihydro-2-isopropyliminophenazine were identified in an initial investigation of its metabolism in leprosy patients. Based on mass, UV and visible spectrometry, an unconjugated (metabolite 1, 3-(p-hydroxyanilino)-10-(p-chlorophenyl)-2,10-dihydro-2-isopropyliminophenazine) and a conjugated (metabolite II, 3-(.beta.-D-glucopyranosiduronic acid)-10-(p-chlorophenyl)-2,10-dihydro-2-isopropyliminophenazine) metabolite were characterized from the urine of patients. Both metabolites were red in color, similar to clofazimine; both were considerably more polar than the parent drug. Metabolite I was apparently formed by a hydrolytic dehalogenation reaction and metabolite II by hydrolytic deamination followed by glucuronidation.

This publication has 1 reference indexed in Scilit: