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The influence of food on the disposition of the antiepileptic oxcarbazepine and its major metabolites in healthy volunteers
Author(s) -
Degen P. H.,
Flesch G.,
Cardot J.M.,
Czendlik C.,
Dieterle W.
Publication year - 1994
Publication title -
biopharmaceutics and drug disposition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.419
H-Index - 58
eISSN - 1099-081X
pISSN - 0142-2782
DOI - 10.1002/bdd.2510150609
Subject(s) - oxcarbazepine , tolerability , pharmacokinetics , pharmacology , anticonvulsant , metabolite , plasma concentration , antiepileptic drug , oral administration , medicine , active metabolite , chemistry , epilepsy , carbamazepine , adverse effect , psychiatry
Abstract The effect of food on the pharmacokinetics of the antiepileptic oxcarbazepine (OXC) was investigated in healthy volunteers. Six healthy male volunteers were treated with single peroral doses of 600 mg of oxcarbazepine (Trileptal®) after overnight fasting or a fat‐ and protein‐rich breakfast. Mean (± SD) areas under the plasma concentration—time curves (AUC) of the major component in plasma, the active monohydroxy metabolite (MHD), which is responsible for the therapeutic effect in man, were 672 (25) μmol L −1 h when given to the fasted volunteers and 780 (31) μmol L −1 h ( p = 0.042) when given after a substantial breakfast. Mean (± SD) maximum concentrations ( C max ) were 25.5 (4.8) μmol L −1 when given to the fasted volunteers and 31.4 (5.3) μmol L −1 ( p = 0.025) when given after breakfast. Thus, the average AUC was increased by 16% and C max by 23% when oxcarbazepine was given with food. The times at which C max was reached ( t max ) as well as the terminal half‐lives were not influenced by concomitant intake of food. The tolerability was the same whether oxcarbazepine was given before or after food in healthy volunteers. The slight effect of food on the kinetics of oxcarbazepine should be of little therapeutic consequence.