Title: Metabolic studies of tolbutamide in the rat
Abstract: Hydroxymethyltolbutamide was found to be the major oxidation product in the urine of rat and rabbit given tolbutamide. The metabolite was identified by its infrared spectrum and by paper and thin-layer chromatography. The enzyme system responsible for the oxidation of tolbutamide is a typical microsomal drug-metabolizing system subject to induction by 3,4-benzpyrene, phenobarbital, and tolbutamide itself. The only product observed after incubating tolbutamide with either the fortified microsomes or with liver homogenate was hydroxymethyltolbutamide. Only a small isotope effect was seen in the oxidation of trideuterated tolbutamide. Hydroxymethyltolbutamide was approximately half as active as tolbutamide in its hypoglycemic activity in mice.
Publication Year: 1967
Publication Date: 1967-01-01
Language: en
Type: article
Indexed In: ['crossref']
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Cited By Count: 50
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