The pharmacokinetics of oxcarbazepine and its active metabolite 10-hydroxy-carbazepine in healthy subjects and in epileptic patients treated with phenobarbitone or valproic acid

Br J Clin Pharmacol. 1993 Oct;36(4):366-8. doi: 10.1111/j.1365-2125.1993.tb00378.x.

Abstract

The kinetics of oxcarbazepine (OXC) and its active metabolite 10-hydroxy-carbazepine (10-OH-CZ) after a single oral OXC dose (600 mg) were compared in healthy control subjects and in epileptic patients treated with phenobarbitone or sodium valproate (n = 8 in each group). In all groups, serum 10-OH-CZ concentrations were much higher than those of the parent drug. In patients on valproate, the kinetics of OXC and 10-OH-CZ did not differ significantly from those observed in controls. In patients on phenobarbitone, AUC values of both OXC and 10-OH-CZ were lower than in controls (2.9 +/- 0.4 vs 5.1 +/- 0.7 microg ml(-1) h and 89 +/- 7 vs 119 +/- 10 microg ml(-1) h respectively, means +/- s.e. mean, P < 0.05), whereas 10-OH-CZ half-lives were only marginally shorter (17 +/- 1 h vs 20 +/- 2 h, NS). These data indicate that the biotransformation of OXC and 10-OH-CZ may be accelerated by concomitant treatment with phenobarbitone but that the magnitude of this effect is unlikely to be of great clinical significance.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Administration, Oral
  • Adult
  • Anticonvulsants / blood
  • Anticonvulsants / pharmacokinetics*
  • Anticonvulsants / therapeutic use
  • Carbamazepine / analogs & derivatives*
  • Carbamazepine / blood
  • Carbamazepine / pharmacokinetics*
  • Drug Interactions
  • Epilepsy / drug therapy
  • Epilepsy / metabolism
  • Female
  • Half-Life
  • Humans
  • Male
  • Oxcarbazepine
  • Phenobarbital / therapeutic use
  • Valproic Acid / therapeutic use

Substances

  • 10,11-dihydro-10-hydroxycarbamazepine
  • Anticonvulsants
  • Carbamazepine
  • Valproic Acid
  • Oxcarbazepine
  • Phenobarbital