抗癫痫药物的分类、作用机制与不良反应

吴冬燕*朱国行**

（复旦大学附属华山医院神经内科 上海 200040）

摘 要抗癫痫药物按作用机制可分为膜稳定剂、减少神经递质释放的药物、提高γ-氨基丁酸能的药物和其他4类。许多抗癫痫药物的作用机制复杂，致使临床中治疗药物的选择及其不良反应均存在不确定性。有些抗癫痫药物有肝酶诱导或抑制作用，故在多药联合治疗或与其他药物合并使用时的代谢速率发生改变。临床上应注意抗癫痫药物的非特异性不良反应，如困倦、头晕等；也应注意各种抗癫痫药物治疗的比较严重的特异性不良反应，如拉莫三嗪可引起严重皮疹、卡马西平会引起白细胞计数降低等。

关键词癫痫 抗癫痫药物 作用机制 不良反应

Classification, mechanism and adverse effects of antiepileptic drugs

WU Dongyan*, ZHU Guoxing**

(Department of Neurology, Huashan Hospital, Fudan University, Shanghai 200040, China)

ABSTRACTAccording to drug mechanism, antiepileptic drugs can be divided into four groups: membrane stabilization, reducing neurotransmitters release, increasing γ-aminobutyric acid mediated inhibition, and the others. Many antiepileptic drugs have more than one mechanism, leading to the uncertainty of drug selection and adverse effects. Some antiepileptic drugs are liver enzyme inducers or inhibitors, resulting in changes in the metabolism, when used in multiple treatment or in combination with other drugs. Antiepileptic drugs have not only non-specific side effects such as drowsiness and dizziness, but also a variety of specific serious adverse effects such as severe rashes caused by lamotrigine and leukopenia caused by carbamazepine.

KEY WORDSepilepsy; antiepileptic drugs; mechanism; adverse effects

抗癫痫药物的化学结构和作用机制各异，且人们对其临床效用和作用机制之间的相互关系还不完全了解，有些作用机制相似的抗癫痫药物的临床效用却存在着较大的差异。额外的作用机制虽可增强抗癫痫药物的疗效，但同时也可能增加不良反应。

1 作用机制与分类

依据作用机制，抗癫痫药物可分为：①膜稳定剂，如钠、钾通道阻滞剂；②减少神经递质释放的药物，如N/P/Q型钙通道阻滞剂和突触囊泡蛋白2A（synaptic vesicle protein 2A, SV2A）配体；③提高γ-氨基丁酸（γ-aminobutyric acid, GABA）介导的兴奋性抑制的药物，如GABA类似物；④其他，如N-甲基-D-天冬氨酸（N-methyl-D-aspartate, NMDA）受体阻滞剂等。各种抗癫痫药物的作用机制归纳见表1。

2 药理学与药代动力学

已发现有些抗癫痫药物作用于目标通道或受体，如钠、钾通道或GABA受体复合体。……