Department of Neurology, Johns Hopkins School of Medicine, Baltimore, MD 21287, USA.
Ann Med. 2012 Nov;44(7):674-9. doi: 10.3109/07853890.2011.603700. Epub 2012 Mar 1.
Lacosamide is a third-generation antiepilepsy drug approved for adjunctive treatment of partial-onset seizures in adults. The pharmacology of lacosamide includes linear kinetics, complete bioavailability, and no major drug interactions. Lacosamide produces slow inactivation of neuronal sodium channels, which differentiates it from other sodium channel modulators, such as carbamazepine and phenytoin. The drug was effective with no major safety problems detected in three large placebo-controlled pivotal trials and has been released in Europe and the US at 200-400 mg/day, divided b.i.d.; an intravenous formulation is approved for temporary conversion from oral therapy. This article reviews the clinical development, pharmacology, and uses of lacosamide for treating partial-onset seizures in adults.
拉科酰胺是一种第三代抗癫痫药物，被批准作为成人部分发作性癫痫的辅助治疗药物。拉科酰胺的药理学特征包括线性药代动力学、完全生物利用度和无主要药物相互作用。拉科酰胺可使神经元钠通道缓慢失活，这使其有别于其他钠通道调节剂，如卡马西平和苯妥英。在三项大型安慰剂对照关键试验中，该药疗效确切，未发现重大安全性问题，已在欧洲和美国上市，剂量为 200-400mg/天，分两次服用；静脉制剂也被批准用于临时转为口服治疗。本文综述了拉科酰胺治疗成人部分发作性癫痫的临床开发、药理学和用途。
