抗癫痫新药左乙拉西坦的临床应用和安全性  

Newer antiepileptic drug levetiracetam:clinical application and safety

作　　者：丁庆明[1] 任连坤[2] 

机构地区：[1]中日友好医院药学部,北京100029 [2]中日友好医院神经内科,北京100029

出　　处：《药物不良反应杂志》2007年第4期295-301,共7页Adverse Drug Reactions Journal

摘　　要：左乙拉西坦(levetiracetam)为吡拉西坦的类似物,是一种新型抗癫痫药,用于部分性发作、肌阵挛发作及原发性全身性强直-阵挛发作的辅助治疗(加用于其他抗癫痫药)。左乙拉西坦口服吸收迅速而完全,血浆药物浓度达峰时间为1.3h。其生物利用度不受食物影响,与血浆蛋白结合率<10%,消除半衰期约为6～8h。成人治疗第1天的初始剂量为1g/d,分2次服用;之后,每2～4周增加1g/d,直至有效控制癫痫发作,最大剂量为3g/d。左乙拉西坦的常见不良反应为嗜睡、无力、头晕。肾功能损害患者及严重肝损害患者使用左乙拉西坦应谨慎并减低剂量。停用左乙拉西坦时应逐渐减量(每2～4周减少1g/d),突然停用易增加癫痫发作频次。Levetiracetam, an analogue piracetam, is one of newer antiepileptic drugs used as adjunctive therapy （added to other antiepileptic drugs） of partial seizures, myoclonic seizures, and primary generalized tonic-clonic seizures. Levetiracetam is rapidly and almost completely absorbed after oral administration, and peak plasma concentration are usually achieved within 1.3 hours. The extent ofbioavailability of levetiracetam is not affected by food. Levetiracetam is less than 10% bound to plasma proteins. Plasma half-life of levetiracetam is approximately 6~8 hours. The initial adult dose is 1 g in two divided doses on the first day of treatment, thereafter, the daily dose may be adjusted in increments of 1 g every 2 to 4 weeks until effective antiepileptic control is achieved, up to a maximum dose of 3 g daily. The most common adverse reactions to levetiracetam are somnolence, weakness, and dizziness. Levetiracetam should be used with caution and in reduced doses in patients with renal impairment and in patients with severe hepatic impairment. Withdrawal of levetiracetam therapy should be made gradually （reducing the daily dose by 1 g every 2 to 4 weeks）, sudden withdrawal may induce an increase in the frequency of seizures.

关 键 词：左乙拉西坦 临床应用 安全性 

分 类 号：R96[医药卫生—药理学]