Effect of phenobarbital on the pharmacokinetics of carbamazepine-10,11-epoxide, an active metabolite of carbamazepine

Ther Drug Monit. 1991 Mar;13(2):109-12. doi: 10.1097/00007691-199103000-00004.

Abstract

The single oral dose kinetics of carbamazepine-10,11-epoxide (CBZ-E), the active metabolite of carbamazepine, were studied in six epileptic patients, stabilized on phenobarbital (PB) monotherapy, and in six drug-free health volunteers. The epoxide metabolite was administered as an enteric-coated tablet at the dose of 200 mg to the patients and at the dose of 100 mg to the volunteers. Patients had a significantly higher plasma clearance of CBZ-E than the control group (mean values +/- SD = 220.2 +/- 63.5 versus 112.5 +/- 46.0 ml/h/kg, p less than 0.007) and a significantly shorter plasma half-life (mean values +/- SD = 4.3 +/- 1.0 versus 6.7 +/- 0.8 h, p less than 0.0015). These results suggest that PB induces CBZ-E metabolism.

MeSH terms

  • Adult
  • Biological Availability
  • Carbamazepine / analogs & derivatives*
  • Carbamazepine / pharmacokinetics
  • Drug Interactions
  • Epilepsy / drug therapy
  • Humans
  • Male
  • Middle Aged
  • Phenobarbital / pharmacology*
  • Phenobarbital / therapeutic use

Substances

  • Carbamazepine
  • carbamazepine epoxide
  • Phenobarbital