Oxcarbazepine disposition: preliminary observations in patients.
We describe a preliminary retrospective study based on the concentration of two hydroxylated metabolites of oxcarbazepine (OCZ), a new anticonvulsant substance, measured in the plasma of 15 patients with epilepsy. Their ages ranged from 8 to 68 years, 6 of them also received phenobarbital and/or phenytoin as co-medication. The concentration of 10-hydroxy-10,11-dihydrocarbamazepine (HCBZ) or of trans-10,11-dihydroxy-10,11-dihydrocarbamazepine (DHCBZ), the metabolites measured, are significantly correlated with the dose of OCZ (p less than 0.05 and p less than 0.01, respectively). DHCBZ concentrations, standardized to a constant OCZ dose or to a constant HCBZ concentration, are significantly higher during co-medication (p less than 0.01 and p less than 0.05, respectively); HCBZ levels are unaffected. These results confirm that enzyme-inducing drugs, although accelerating the oxidation HCBZ, do not induce its formation. Since HCBZ is the active metabolite, such drug interaction seems unlikely to alter OCZ pharmacological activity.
Kumps
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A
Free University of Brussels (ULB), Pharmaceutical Institute, Belgium.
Wurth
C
C
D000293:Adolescent; D000328:Adult; D000368:Aged; D000927:Anticonvulsants / Q000378:metabolism / Q000493:pharmacokinetics*; D002220:Carbamazepine / Q000031:analogs & derivatives* / Q000378:metabolism / Q000493:pharmacokinetics*; D002648:Child; D004347:Drug Interactions; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D000078330:Oxcarbazepine; D010634:Phenobarbital / Q000494:pharmacology; D010672:Phenytoin / Q000494:pharmacology
C000612069:10-hydroxy-10,11-dihydrocarbamazepine; D000927:Anticonvulsants; D002220:Carbamazepine; D010672:Phenytoin; D000078330:Oxcarbazepine; D010634:Phenobarbital