Department of Neurology, Barrow Neurological Institute, St. Joseph's Hospital and Medical Center, Phoenix, Arizona 85013, USA.
Expert Opin Pharmacother. 2010 Jun;11(9):1595-602. doi: 10.1517/14656566.2010.488639.
Epilepsy is one of the most common neurological disorders, affecting up to 2% of the population worldwide. Studies show that patients with refractory seizures have higher morbidity and mortality rates, as well as a poorer quality of life, than those with controlled seizures. Therefore, treatment that reduces the frequency of seizures may improve patients' quality of life. Lacosamide (LCM) is a recently approved anticonvulsant in Europe and the USA which offers new mechanisms of action and favorable safety profiles. Efficacy data have shown fast onset of anticonvulsant effects and significant reduction of partial-onset seizures as adjunctive therapy at LCM 200 and 400 mg/day, even in a severely refractory population.
This article reviews three pivotal clinical trials of LCM, including its efficacy and tolerability over 7 years. In addition, LCM's key pharmacodynamics and pharmacokinetics from a search of the literature are reviewed in detail. This article also includes recent publications on the safety and use of intravenous LCM solution for patients with epilepsy.
This article provides comprehensive review of efficacy and safety information of LCM along with comprehensive pharmacokinetic information, which includes absolute bioavailability, low protein binding, lack of hepatic enzyme induction or inhibition, and low potential for drug-drug interactions.
Considering the fact that more than 30% of epilepsy patients remain refractory despite various antiepileptic drugs, LCM may provide added benefit to patients with refractory seizures.
癫痫是最常见的神经障碍之一,影响全球多达 2%的人口。研究表明,难治性癫痫发作的患者比控制良好的癫痫发作患者具有更高的发病率和死亡率,以及更差的生活质量。因此,减少癫痫发作频率的治疗可能会改善患者的生活质量。拉考沙胺 (LCM) 是一种最近在欧洲和美国获得批准的抗癫痫药,具有新的作用机制和良好的安全性。疗效数据表明,LCM 200 和 400mg/天的辅助治疗具有快速抗惊厥作用,并且可显著减少部分发作性癫痫发作,即使在严重难治性人群中也是如此。
本文综述了 LCM 的三项关键性临床试验,包括其 7 年的疗效和耐受性。此外,还详细回顾了文献中搜索到的 LCM 的关键药代动力学和药效学。本文还包括最近关于癫痫患者使用静脉内 LCM 溶液的安全性和用途的出版物。
本文提供了 LCM 的疗效和安全性信息的全面综述,以及全面的药代动力学信息,包括绝对生物利用度、低蛋白结合、缺乏肝酶诱导或抑制以及低药物相互作用潜力。
鉴于超过 30%的癫痫患者尽管使用了各种抗癫痫药物仍存在难治性,LCM 可能为难治性癫痫发作的患者提供额外的益处。