非氨酯与其他几种抗癫痫药物对小鼠最大电休克诱导惊厥的相互作用。

Interaction of felbamate with several other antiepileptic drugs against seizures induced by maximal electroshock in mice.

作者信息

Gordon R, Gels M, Wichmann J, Diamantis W, Sofia R D

机构信息

Wallace Laboratories, Division of Carter-Wallace, Cranbury, New Jersey 08512.

出版信息

Epilepsia. 1993 Mar-Apr;34(2):367-71. doi: 10.1111/j.1528-1157.1993.tb02423.x.

DOI:10.1111/j.1528-1157.1993.tb02423.x

PMID:8453946

Abstract

The anticonvulsant effects of felbamate (FBM) alone or in combination with phenytoin (PHT), carbamazepine (CBZ), valproate (VPA), or phenobarbital (PB) were investigated against maximal electroshock (MES) seizures in mice. Nonprotective doses of the prototype antiepileptic drugs (AEDs) enhanced the protective effects of FBM against electrically induced seizures, as shown by significant reduction of FBM ED50 values. Toxicity as determined by rotorod test was not significantly potentiated, however, and the protective index (PI = TD50/ED50) of FBM was increased by > 100% for each AED interaction. The increase in anticonvulsant potency of FBM after its combination with nonprotective doses of AEDs could not be accounted for by a pharmacokinetic mechanism.

摘要

研究了非氨酯（FBM）单独或与苯妥英（PHT）、卡马西平（CBZ）、丙戊酸盐（VPA）或苯巴比妥（PB）联合使用对小鼠最大电休克（MES）惊厥的抗惊厥作用。如FBM半数有效剂量（ED50）值显著降低所示，原型抗癫痫药物（AEDs）的非保护剂量增强了FBM对电诱导惊厥的保护作用。然而，通过转棒试验测定的毒性并未显著增强，并且每种AED相互作用使FBM的保护指数（PI = TD50/ED50）提高了100%以上。FBM与非保护剂量的AEDs联合后抗惊厥效力的增加不能用药物代谢动力学机制来解释。