抗癫痫新药哌拉帕纳的药理作用与临床评价

Pharmacological and clinical evaluation of a new antiepilepsia drug,perampanel

哌拉帕纳为非竞争性谷氨酸受体突触后神经元拮抗剂,用于12岁及以上伴有或无继发性全身性癫痫的部分性癫痫发作的辅助治疗,于2012年10月22日由美国FDA批准上市,其确切的抗癫痫机制尚未完全清楚,其常见不良反应包括头晕、步态不稳、睡意、疲乏、易怒、跌跤、恶心、体重增加、共济失调和平衡障碍。本文对哌拉帕纳的药理作用、药动学、药物相互作用、临床评价和安全性等进行介绍。

Perampanel, a non-competitive antagonist of AMPA glutamate receptor on post-synaptic neu- rons, is indicated as adjunctive therapy for the treatment of partial-onset seizures with or without secondarily general- ized seizures in patients with epilepsy aged 12 years and older. It was approved by the U. S. Food and Drug Admin- istration on October 22,2012. The precise mechanism by which perampanel exerts its antiepileptic effects in hu- mans has not been fully elucidated. The most common adverse reactions were dizziness, somnolence, fatigue, irri- tability, falls, nausea, ataxia, balance disorder, gait disturbance, vertigo and weight gain,etc. The pharmacology, pharmacokinetics, drug interactions, clinical evaluation and safety of perampanel were reviewed in this paper.