May T W, Rambeck B, Sälke-Kellermann A
Department of Biochemistry, Gesellschaft für Epilepsieforschung e.V., Bethel, Bielefeld, Germany.
Acta Neurol Scand. 1996 Jun;93(6):393-7. doi: 10.1111/j.1600-0404.1996.tb00016.x.
Oxcarbazepine (OCBZ) is a new antiepileptic drug with a chemical structure similar to carbamazepine. We investigated the daily fluctuations of 10-OH-carbazepine (monohydroxy derivative, MHD), the clinically relevant metabolite of OCBZ, in patients with or without comedication. Twenty-two profiles of (total) serum concentrations of MHD from 18 epileptic patients on a b.i.d. OCBZ regimen were determined at 8.00, 11.00, 14.00, 17.00, 20.00 h (and 22.00 h/23.00 h). A patient was only considered twice if his comedication or OCBZ dosage had been changed. The maximal MHD concentrations were about 33% +/- 14% higher than the minimal MHD concentrations during the day. The free MHD concentrations were determined in 17 profiles. The mean free fraction of MHD was 56.7% +/- 5.5%. In combination with valproic acid the free fraction (64.0% +/- 1.4%) was slightly, but significantly higher (p < 0.05) than in monotherapy (52.3% +/- 0.9%) or in combination (58.0% +/- 2.6%) with other antiepileptic drugs (2 x phenobarbital, 2 x methsuximide, 1 x sulthiame). Further studies are necessary to clarify if the observed fluctuations of MHD are of clinical importance.
奥卡西平（OCBZ）是一种新型抗癫痫药物，其化学结构与卡马西平相似。我们研究了有或无合并用药的患者中奥卡西平的临床相关代谢产物10-羟基奥卡西平（单羟基衍生物，MHD）的每日波动情况。对18例接受奥卡西平每日两次给药方案的癫痫患者的MHD（总）血清浓度进行了22次监测，监测时间点为8:00、11:00、14:00、17:00、20:00时（以及22:00/23:00时）。仅当患者的合并用药或奥卡西平剂量发生变化时才会对其进行两次监测。白天MHD的最大浓度比最小浓度高约33%±14%。对17次监测结果测定了游离MHD浓度。MHD的平均游离分数为56.7%±5.5%。与丙戊酸合用时，游离分数（64.0%±1.4%）略高于单药治疗（52.3%±0.9%）或与其他抗癫痫药物（2次与苯巴比妥合用、2次与甲琥胺合用、1次与舒噻美合用）合用时的游离分数（58.0%±2.6%），且差异有统计学意义（p<0.05）。有必要进一步研究以明确观察到的MHD波动是否具有临床意义。
