Metabolism of 14C-3-trifluoromethyl-alpha-ethylbenzhydrol in rats.

Metabolism of 3-trifluoromethyl-alpha-ethyl-benzhydrol (I), hepatic enzyme inducer has been studied in rats. Five metabolites in bile and four in urine, as well as minute amounts of the original drug (I) were identified. The only major metabolite in bile and one of the two major metabolites in urine were found to be aromatic hydroxylated products of I, i.e., 3-trifluoro-methyl-4'-hydroxy-alpha-ethylbenzhydrol (II). The results of enzymatic hydrolysis with beta-glucuronidase/arylsulfatase suggest that hydroxyl groups of metabolites are conjugated. Considering the structure of metabolites isolated a probable order of metabolite formation is outlined.