Ben-Menachem Elinor
Institute of Clinical Neurosciences, Division of Neurology, Sahlgrenska Academy, Göteborg University, Göteborg, Sweden.
Drugs Today (Barc). 2008 Jan;44(1):35-40. doi: 10.1358/dot.2008.44.1.1178468.
Lacosamide, (R)-2-acetamido-N-benzyl-3-meth- oxypropionamide, is a new chemical entity specifically synthesized as an anticonvulsive drug candidate, which appears to have a novel dual mode of action. Its pharmacokinetic characteristics have been studied in young and elderly healthy adults, as well as in adults with epilepsy or diabetic neuropathic pain. After oral administration, lacosamide is rapidly and completely absorbed. An elimination half-life of 13 hours allows for twice-daily dosing. Lacosamide has a low potential for drug-drug interactions. Both oral and intravenous formulations of lacosamide are being developed. In completed placebo-controlled clinical trials, lacosamide has demonstrated efficacy as adjunctive therapy for reduction of seizure frequency in patients with uncontrolled partial-onset seizures, and has been generally well tolerated. For patients treated with lacosamide, the most frequently reported adverse events in placebo-controlled trials include dizziness, headache, nausea and diplopia. When used as short-term replacement for oral lacosamide, intravenous lacosamide has a comparable safety profile to oral lacosamide. Results from clinical trials to date suggest that lacosamide may be a useful pharmacological treatment option for patients with partial-onset seizures.
拉科酰胺,即(R)-2-乙酰氨基-N-苄基-3-甲氧基丙酰胺,是一种专门合成的新型化学实体,作为抗惊厥药物候选物,似乎具有一种新的双重作用模式。其药代动力学特征已在年轻和老年健康成年人以及患有癫痫或糖尿病性神经病理性疼痛的成年人中进行了研究。口服给药后,拉科酰胺迅速且完全吸收。13小时的消除半衰期允许每日给药两次。拉科酰胺发生药物相互作用的可能性较低。拉科酰胺的口服和静脉制剂均在研发中。在已完成的安慰剂对照临床试验中,拉科酰胺已证明作为辅助疗法可降低部分性发作未得到控制的患者的癫痫发作频率,并且总体耐受性良好。对于接受拉科酰胺治疗的患者,在安慰剂对照试验中最常报告的不良事件包括头晕、头痛、恶心和复视。当用作口服拉科酰胺的短期替代药物时,静脉注射拉科酰胺的安全性与口服拉科酰胺相当。迄今为止的临床试验结果表明,拉科酰胺可能是部分性发作患者有用的药物治疗选择。