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Lacosamide for the prevention of partial onset seizures in epileptic adults

机译:Lacosamide预防癫痫成人的部分发作

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摘要

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.
机译:Lacosamide是一种新注册的具有双重作用机制的抗癫痫药。它选择性地增强了电压门控性钠通道的缓慢灭活,从而导致了过度兴奋性神经元膜的稳定和对重复性神经元放电的抑制。它还与折叠反应介体蛋白2 CRMP2结合。 Lacosamide具有良好的药代动力学特性;被迅速完全吸收,消除半衰期相对较长,为13小时,允许每天两次给药,线性药代动力学,药物相互作用和消除肾脏的可能性低。拉可酰胺的口服和静脉内制剂都在开发中。在安慰剂对照的临床试验中,对于未控制的部分发作的癫痫患者,拉考酰胺可有效减少癫痫发作作为辅助治疗。 Lacosamide一般耐受良好。在安慰剂对照试验中,最常报告的不良事件是头晕,头痛,恶心和复视。静脉内拉可酰胺具有相当好的安全性。

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