左乙拉西坦基础研究进展

Progress of Levetiracetam Basic Research

目的介绍新型抗癫痫药物左乙拉西坦(LEV)基础动物实验研究方面的进展。方法通过查阅近年来的报道,概括了LEV作用于癫痫动物模型的机制、以及与癫痫耐药相关蛋白、脑保护的关系。结果 LEV具有与既往抗癫痫药物不同的作用机制,不仅有抗癫痫作用,还具有抑制癫痫源产生和发展的作用。多数报道LEV不是常见耐药蛋白如P-gp和MRP1/2,MDR1的底物,在难治性癫痫的治疗中具有理论基础,同时LEV在神经保护方面急性期多具积极作用,而在慢性期效果不明显。结论大量动物实验证明LEV具有全新的作用机制,对于临床癫痫的治疗具有重要指导意义,但在不同癫痫模型及组织中结果不尽相同,值得进一步探讨,为开发新的抗癫痫药物提供借鉴。

OBJECTIVE To introduce the progress study of the new antiepileptic drug of levetiracetam in basic animal experiments. METHODS By investigating the international literatures in recent years, we summed up the role of levetiracetam mechanism in epilepsy animal models, and the relationship with epilepsy drug resistance protein, brain protection. RESULTS LEV has different mechanisms with previously antiepileptic drugs, which not only has antiepileptic effects, also has the role of suppressing the generation and development of epilepsy. According to the most reports that LEV is not a substrate of common drug resistance proteins such as P-gp, MRP1/2 and MDR1, in treatment of refractory epilepsy has a theoretical foundation, meanwhile LEV has more neuroprotective in acute phase of epilepsy model, not in the chronic period. COCLUSION A large number of animal experiments show that LEV has a completely new mechanism, for the clinical treatment of epilepsy has important guiding significance, but the results are different in different epilepsy models or organization which needs to be further investigated, to provide a reference for the development of new anti-epileptic drugs.