THE INFLUENCE OF FOOD ON THE DISPOSITION OF THE ANTIEPILEPTIC OXCARBAZEPINE AND ITS MAJOR METABOLITES IN HEALTHY-VOLUNTEERS

The effect of food on the pharmacokinetics of the antiepileptic oxcarb azepine (OXC) was investigated in healthy volunteers. Six healthy male volunteers were treated with single peroral doses of 600 mg of oxcarb azepine (Trileptal(R)) after overnight fasting or a fat- and protein-r ich 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 m an, were 672 (25) mu mol L(-1) h when given to the fasted volunteers a nd 780 (31) mu mol L(-1) h (p = 0.042) when given after a substantial breakfast. Mean (+/-SD) maximum concentrations (C-max) were 25.5 (4.8) mu mol L(-1) when given to the fasted volunteers and 31.4(5.3) mu mol L(-1) (p = 0.025) when given after breakfast. Thus, the average AUC wa s 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 ter minal half-lives were not influenced by concomitant intake of food. Th e tolerability was the same whether oxcarbazepine was given before or after food in healthy volunteers. The slight effect of food on the kin etics of oxcarbazepine should be of little therapeutic consequence.