左乙拉西坦——一种具有全新作用机制的抗癫痫新药  

Levetiracetam——a novel antiepileptic drug with a unique preclinical profile

作　　者：田国红[1] 赵忠新[1] 

机构地区：[1]中国人民解放军上海第二军医大学附属长征医院神经内科,上海200003

出　　处：《中国新药与临床杂志》2006年第10期782-786,共5页Chinese Journal of New Drugs and Clinical Remedies

摘　　要：左乙拉西坦是一种新型的口服抗癫痫药物,与其他抗癫痫药物的结构不同,具有全新的抗癫痫机制。左乙拉西坦的确切抗癫痫机制尚不明,但与传统抗癫痫药物作用于离子通道或兴奋性、抑制性神经递质系统不同。左乙拉西坦几乎具备了较好的抗癫痫药物的所有药动学特性:生物利用度高、线性曲线、低蛋白结合率、无肝酶诱导作用。多种动物模型显示左乙拉西坦具有抗癫痫特性。全球范围的3个重要多中心、随机、双盲、安慰剂对照临床试验结果显示左乙拉西坦具有确切的抗癫痫疗效和很好的耐受性,可用于治疗癫痫、神经痛和其他神经系统疾病。Levetiracetam （Lev） is a novel orally active antiepileptic drug, structurally unrelated to other antiepileptics and with an entirely unique preclinical profile. The precise mechanisms of its antiepileptic effect is unknown and does not appear to derive from any ion passage interaction with known mechanisms involved in inhibitory and excitable neurotransmission. The pharmacokinetic profile of Lev closely approximates the ideal characteristics expected of an antiepileptic drug, with good bioavailability, linear and time-invariant kinetics, minireal protein binding, and least metabolism. The antiepileptic activity of Lev was assessed in a number of animal models ereated for investigation of epileptic： seizures. The effectiveness of Lev was confirmed and revealed in three pivotal muhicenter, randomized, double-blind, and placebo-controlled clinical trials conducted in the United States and Europe that Lev is well tolerable and safe for patients with seizure, cognitive, and anxiety disorders.

关 键 词：药动学 药物疗法 安全 抗癫痫药物 左乙拉西坦 

分 类 号：R971.6[医药卫生—药品]