METABOLISM OF CARBAMAZEPINE AND ITS EPOXIDE METABOLITE IN HUMAN AND RAT-LIVER INVITRO

  • 1 January 1981
    • journal article
    • research article
    • Vol. 9  (6) , 561-564
Abstract
The epoxidation of carbamazepine (CBZ) [an anticonvulsant] and the hydration of the primary epoxide metabolite was studied in microsomes isolated from 10 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 specimens in the activity of both enzymes. There appeared to be a positive correlation between the activity of the 2 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 the epoxidation.

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