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It i8 shown that chlorpropamide, previously thought to be a nonmetabolized drug, undergoes metabolic transformation in man. Two of the metabolites were identified by chromatographic techniques as p-chlorobenzenesulfonylurea and p-chlorobenzenesulfonamide. Estimation of the quantities of these metabolites and of unchanged chlorpropamide in the urine of diabetic patients showed that a considerable quantity of an unidentified metabolite must also be excreted. The proportion of the drug converted to the two identified metabolites varies in different individuals on long-term chlorpropamide therapy. A modified plasma assay procedure for chlorpropamide which reduces interference from metabolites is described.

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