M. A. Schwartz, E. Postma
1972
Citations
0
Influential Citations
22
Citations
Quality indicators
Journal
Journal of pharmaceutical sciences
Abstract
The biotransformation of demoxepam, 7-chloro-1,3-dihydro-5-phenyl-2H-1,4-benzodiazepin-2-one 4-oxide, was studied in two subjects. Following the administration of a 20-mg. oral dose of demoxepam-2-14C, these subjects excreted 24 and 29% of the dose in the urine as unchanged drug. The urinary metabolites included “opened lactam” (formed by hydrolysis of the lactam bond), conjugated oxazepam (N-desoxy-3-hydroxydemoxepam), and two conjugated phenols, the 5-(4-hydroxyphenyl) derivative (I) and the 9-hydroxy derivative (II) of demoxepam. N-Desoxydemoxepam, an apparent intermediate in the formation of oxazepam, was the only metabolite identified in the feces. Of these metabolites, only opened lactam was previously shown to be a metabolite of chlordiazepoxide in man.