National Institute of Neurosciences, Epilepsy Center, 1145 Budapest, Amerikai út 57, Hungary.
Neuropsychiatr Dis Treat. 2010 Sep 7;6:465-71. doi: 10.2147/ndt.s7967.
Lacosamide is a newly registered antiepileptic drug with dual mechanisms of action. It selectively enhances slow inactivation of voltage-gated sodium channels, resulting in stabilization of hyperexcitable neuronal membranes and inhibition of repetitive neuronal firing. It also binds to a collapsing-response mediator protein-2, CRMP2. Lacosamide has a favorable pharmacokinetic profile; is rapidly and completely absorbed, has a relatively long elimination half-life of 13 hours which allows twice-daily administration, linear pharmacokinetics, and has low potential for drug interactions and renal elimination. Both oral and intravenous formulations of lacosamide are being developed. In placebo-controlled clinical trials, lacosamide was effective in seizure reduction as adjunctive therapy in patients with uncontrolled partial-onset seizures. Lacosamide was generally well tolerated. The most frequently reported adverse events in placebo-controlled trials were dizziness, headache, nausea, and diplopia. Intravenous lacosamide has a comparably good safety profile.
拉科酰胺是一种新注册的抗癫痫药物,具有双重作用机制。它选择性地增强电压门控钠离子通道的缓慢失活,从而稳定过度兴奋的神经元膜并抑制神经元的重复放电。它还与崩塌反应介质蛋白-2(CRMP2)结合。拉科酰胺具有良好的药代动力学特性;它被快速且完全吸收,消除半衰期相对较长(13 小时),允许每日给药两次,具有线性药代动力学特征,并且药物相互作用和肾脏消除的潜力较低。拉科酰胺的口服和静脉制剂都在开发中。在安慰剂对照临床试验中,拉科酰胺作为辅助治疗药物,对未控制的部分发作性癫痫发作患者的癫痫发作减少有效。拉科酰胺通常具有良好的耐受性。安慰剂对照试验中报告的最常见不良反应为头晕、头痛、恶心和复视。静脉内拉科酰胺具有类似良好的安全性特征。