Arkansas Epilepsy Program, 2 Lile Court Ste 100, Little Rock, AR 72205, USA.
Expert Rev Neurother. 2012 Jun;12(6):645-55. doi: 10.1586/ern.12.50.
Lacosamide (LCM) is an antiepileptic drug approved as adjunctive therapy for partial-onset seizures in adults. It has a mechanism of action that differs from other antiepileptic drugs in that it selectively enhances sodium channel slow inactivation, which is in contrast to 'traditional' sodium channel blockers (e.g., carbamazepine, oxcarbazepine, lamotrigine and phenytoin) that primarily affect fast inactivation. The pharmacokinetic profile of LCM is well characterized and includes a fast rate of absorption, little or no interaction with cytochrome P450 isoenzymes, limited effect of age and gender on plasma levels, and low potential for drug-drug interactions. Safety and efficacy data from three double-blind, placebo-controlled trials, as well as pooled and post hoc analyses of these three trials, have been published, and demonstrate the safety and rapid-onset efficacy of LCM in adults with treatment-refractory partial-onset seizures. LCM is available in tablets and an intravenous formulation when oral administration is temporarily not feasible.
拉科酰胺（LCM）是一种抗癫痫药物，被批准作为成人部分发作性癫痫的辅助治疗药物。其作用机制与其他抗癫痫药物不同，它选择性地增强钠离子通道缓慢失活，这与“传统”钠离子通道阻滞剂（如卡马西平、奥卡西平、拉莫三嗪和苯妥英）主要影响快速失活形成对比。LCM 的药代动力学特征良好，包括吸收速度快、与细胞色素 P450 同工酶几乎没有相互作用、年龄和性别对血浆水平的影响有限、药物相互作用的潜力低。三项双盲、安慰剂对照试验的安全性和疗效数据，以及这三项试验的汇总和事后分析已经发表，证明了 LCM 在治疗抵抗性部分发作性癫痫成人中的安全性和快速起效疗效。当口服暂时不可行时，LCM 有片剂和静脉注射制剂两种剂型。
