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拉科酰胺:一种用于辅助治疗部分性发作的研究性药物。

Lacosamide: an investigational drug for adjunctive treatment of partial-onset seizures.

作者信息

Ben-Menachem Elinor

机构信息

Institute of Clinical Neurosciences, Division of Neurology, Sahlgrenska Academy, Göteborg University, Göteborg, Sweden.

出版信息

Drugs Today (Barc). 2008 Jan;44(1):35-40. doi: 10.1358/dot.2008.44.1.1178468.

DOI:10.1358/dot.2008.44.1.1178468
PMID:18301802
Abstract

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.

摘要

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。

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Lacosamide: an investigational drug for adjunctive treatment of partial-onset seizures.拉科酰胺:一种用于辅助治疗部分性发作的研究性药物。
Drugs Today (Barc). 2008 Jan;44(1):35-40. doi: 10.1358/dot.2008.44.1.1178468.
2
Lacosamide: an adjunctive agent for partial-onset seizures and potential therapy for neuropathic pain.拉科酰胺:部分发作性癫痫的辅助治疗药物,也是治疗神经病理性疼痛的潜在药物。
Ann Pharmacother. 2009 Nov;43(11):1809-17. doi: 10.1345/aph.1M303. Epub 2009 Oct 20.
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Safety and tolerability of lacosamide as adjunctive therapy for adults with partial-onset seizures: Analysis of data pooled from three randomized, double-blind, placebo-controlled clinical trials.拉科酰胺作为成人部分性发作辅助治疗的安全性和耐受性:来自三项随机、双盲、安慰剂对照临床试验的汇总数据分析
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Long-term safety and efficacy in patients with uncontrolled partial-onset seizures treated with adjunctive lacosamide: results from a Phase III open-label extension trial.拉科酰胺辅助治疗未控制部分发作性癫痫患者的长期安全性和疗效:III 期开放标签扩展试验结果。
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A noninterventional study evaluating the effectiveness and safety of lacosamide added to monotherapy in patients with epilepsy with partial-onset seizures in daily clinical practice: The VITOBA study.一项在日常临床实践中评估拉考酰胺添加到单药治疗对部分性发作癫痫患者有效性和安全性的非干预性研究:VITOBA研究。
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Efficacy and safety of oral lacosamide as adjunctive therapy in adults with partial-onset seizures.口服拉科酰胺作为辅助疗法治疗成人部分性发作癫痫的疗效和安全性。
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Safety and tolerability of adjunctive lacosamide intravenous loading dose in lacosamide-naive patients with partial-onset seizures.在部分发作性癫痫患者中,添加左乙拉西坦静脉负荷剂量的安全性和耐受性。
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Safety and efficacy of adjunctive lacosamide among patients with partial-onset seizures in a long-term open-label extension trial of up to 8 years.在一项长达8年的长期开放标签扩展试验中,拉科酰胺辅助治疗部分性发作患者的安全性和有效性。
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Lacosamide and epilepsy.拉科酰胺与癫痫。
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Pharmacotherapy for Status Epilepticus.癫痫持续状态的药物治疗
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New and emerging treatments for epilepsy: review of clinical studies of lacosamide, eslicarbazepine acetate, ezogabine, rufinamide, perampanel, and electrical stimulation therapy.癫痫的新型及新兴治疗方法:拉科酰胺、醋酸艾司利卡西平、依佐加宾、卢非酰胺、吡仑帕奈及电刺激疗法的临床研究综述
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