2013•Handbook of Metabolic Pathways of XenobioticsRequires access
Tolbutamide
Jiangbo Du
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Abstract
Tolbutamide is an oral hypoglycemic drug used to treat type II diabetes. [14C]‐Tolbutamide metabolites were detected in rat microsomes, including hydroxyl‐tolbutamide, carboxy‐tolbutamide, p‐tolylsulfonylurea, p‐tolylsulfonamide, three monohydroxylated metabolites from the butyl side chain, and two GST‐mediated glutathione conjugates. The metabolic profile of [14C]‐tolbutamide in rats was studied. Three new metabolites, ω‐carboxyl tolbutamide, O‐glucuronide conjugate of hydroxyl‐tolbutamide, and ortho‐ or meta‐tolbutamide glutathione, were detected in rat biological samples, in addition to the metabolites detected in vitro. After oral administration of [3H]‐tolbutamide to male human subjects, metabolites hydroxyl‐tolbutamide and carboxy‐tolbutamide were the radioactive materials detected in urine.