부산대학교 도서관

Oxcarbazepine (OXC) is the keto analogue of carbamazepine (CBZ) and was developed to overcome some of the pharmacological drawbacks of CBZ, while offering identical efficacy. The immediate-release (IR) formulation of OXC was labeled worldwide in 2000 for the treatment of epilepsies with focal seizures with and without secondary generalization both in monotherapy and add-on treatment (Trileptal(r), Novartis Pharma AG Timox(r), Desitin Arzneimittel GmbH). IR OXC has an almost complete bioavailability, is absorbed independently of food and reaches peak serum concentrations within 1--3 hours. OXC is rapidly metabolized to its monohydroxy derivative (MHD), which is the active antiepileptic compound. Serum peak concentrations of MHD are reached within 4--12 hours. The eliminated half-life in healthy subjects is 1--5 hours for OXC and 7--20 hours for MHD, respectively. Modified-release (MR) OXC was labeled in Germany in 2008 (Apydan(r) extent, Desitin Arzneimittel GmbH). In general, one should expect that the switch from IR to MR OXC might be beneficial in terms of tolerability in patients suffering from side effects of high-dose IR OXC, since under steady-state conditions MR OXC flattens the OXC serum concentration peak that may be responsible for effects such as dizziness, vertigo or blurred vision within two hours after oral intake. Clinical experiences are reported in a group of 31 adult patients who complained about such adverse effects with Trileptal(r) or Timox(r) and were switched to Apydan(r) extent. Four patients were on OXC monotherapy, the remaining 27 patients were treated with OXC according to an add-on regimen. After a follow-up of 6--11 months, the switch did not influence efficacy or tolerability of OXC in 8 cases, while tolerability improved in 22 patients. In 3 patients the number of daily dosages could be reduced. Whereas 2 patients complained about more seizures which could be compensated by an increase of OXC, 3 patients became seizure free. These findings demonstrate a potential benefit of MR OXC in a variety of patients.