title: Metabolism of carbamazepine and its epoxide metabolite in human and rat liver in vitro.
abstract: The epoxidation of carbamazepine (CBZ) and the hydration of the primary epoxide metabolite was studied in microsomes isolated from ten human livers. To study the epoxide hydrolase activity a high-performance liquid-chromatographic method was developed for the analysis of dihydro-CBZ-trans-diol. There was a pronounced variation between the specimens in the activity of both enzymes. There appeared to be a positive correlation between the activity of the two enzymes. In rats pretreated with either CBZ or phenobarbital for 4 days, the microsomal epoxidation of CBZ was induced. The epoxide hydrolase activity was also increased, although less so than in epoxidation.
mesh_terms: D000818:Animals; D002220:Carbamazepine / Q000031:analogs & derivatives* / Q000378:metabolism* / Q000494:pharmacology; D004790:Enzyme Induction / Q000187:drug effects; D004851:Epoxide Hydrolases / Q000378:metabolism*; D006801:Humans; D007536:Isomerism; D008297:Male; D008862:Microsomes, Liver / Q000378:metabolism*; D006899:Mixed Function Oxygenases / Q000378:metabolism*; D010634:Phenobarbital / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D013045:Species Specificity
chemical_list: D002220:Carbamazepine; C004822:10,11-dihydro-10,11-dihydroxy-5H-dibenzazepine-5-carboxamide; D006899:Mixed Function Oxygenases; D004851:Epoxide Hydrolases; C012227:carbamazepine epoxide; D010634:Phenobarbital