MECHANISMS OF ACTION OF CURRENTLY PRESCRIBED AND NEWLY DEVELOPED ANTIEPILEPTIC DRUGS

被引:105
作者
MACDONALD, RL [1 ]
KELLY, KM [1 ]
机构
[1] UNIV MICHIGAN,SCH MED,DEPT PHYSIOL,ANN ARBOR,MI
关键词
ANTICONVULSANTS; PHENYTOIN; CARBAMAZEPINE; BARBITURATES; BENZODIAZEPINES; VALPROATE; ETHOSUXIMIDE; LAMOTRIGINE; GABAPENTIN; FELBAMATE;
D O I
10.1111/j.1528-1157.1994.tb05955.x
中图分类号
R74 [神经病学与精神病学];
学科分类号
摘要
Clinically available antiepileptic drugs (AEDs) decrease membrane excitability by interacting with neurotransmitter receptors or ion channels. AEDs developed before 1980 appear to act on sodium (Na) channels, gamma-aminobutyric acid(A) (GABA(A)) receptors, or calcium (Ca) channels. Benzodiazepines and barbiturates enhance GABA(A)-receptor-mediated inhibition. Phenytoin, carbamazepine and, possibly, valproate (VPA) decrease high-frequency repetitive firing of action potentials by enhancing Na channel inactivation. Ethosuximide and VPA reduce a low threshold (T-type) Ca-channel current. The mechanisms of action of recently developed AEDs are less clear. Lamotrigine may decrease sustained high-frequency repetitive firing of voltage-dependent Na action potentials, and gabapentin (GBP) appears to bind to a specific binding site in the CNS with a restricted regional distribution. However, the identity of the binding site and the mechanism of action of GBP remain uncertain. The antiepileptic effect of felbamate may involve interaction at the strychnine-insensitive glycine site of the N-methyl-D-aspartate receptor, but the mechanism of action is not yet proven.
引用
收藏
页码:S41 / S50
页数:10
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