药物的抗惊厥作用

Anticonvulsant Effects of Drugs

XXX

（China Pharmaceutical University，639 Longmian Avenue, Nanjing, Jiangsu, China 210009）

ABSTRACT: OBJECTIVE:To study the anticonvulsant efficacy of Phenytoin sodium and Phenobarbital and valproate on convulsion. METHODS: The anticonvulsant activity of the drugs was evaluated by the maximal electroshock (MES) test and remeflin seizure test. Induced rats were treated by intraperitoneal injection ,then observe the incubation period (up to tails upright 45°) and degree of reaction of each mouse(spasm, falling down ,stiff or death). RESULTS:1. In MES experiment, the degree of convulsion: The Phenobarbital group (P<0.05 vs normal saline group) was the lightest, and the NS group was the severest one. 2. In remeflin experiment, the similar result was observed between valproate group and NS group (P<0.01). CONCLUSION: Phenobarbital has better anti-convulsion effect than Phenytoin sodium on convulsion induced by electroshock, and valproate has a significant effect to anti-convulsion induced by remeflin.

KEYWORDS Phenytoin sodium; Phenobarbital; valproate; remeflin ; anti-convulsion Introduction

Phenytoin sodium: its mechanism of action: It can block sodium channels (voltage-, frequency-, and time dependent fashion) and inhibit the generation of action potentials and It can increase the function of inhibitory transmitter GABA, inhibit nerve terminal to uptake GABA and induce the increasing of GABA receptor, thereby enhance GABA-mediated postsynaptic inhibition.

Phenobarbital: its mechanism of action: Phenobarbital can inhibit the paradoxical discharge of epilepsy focus selectively, enhance stimulation of surrounding tissues and block discharge diffuse to normal tissues and Phenobarbital facilitate GABA-mediated inhibition of neuronal activity.

Valproate is broad spectrum antiepileptic drug, which is used to all types of epilepsy; its mechanism is that enhancing the enzymatic activity of glutamate decarboxylase. And Inhibiting GABA reuptake and synapse inactivation via releasing synapse frontal membrane GABA and then enhance GABA postsynaptic inhibition

Remeflin, a central stimulate which can directly excite respiratory center, can produce convulsion with over-dose. The protective effects of drugs on convulsion produced by remeflin can be used to screen antiepileptic and anti-convulsion.

Stimulating mouse head with a strong electric current can cause general tetanic convulsion. If a drug can prevent the occurrence of general titanic convulsion, we could initially suspect that it has antagonistic effect on grand mal. Remeflin, a central stimulant which can directly excite respiratory center, can protective effects of drugs on convulsion produced by remeflin can be used to screen antiepileptics and anticonvulsants. [1]