Sills Graeme J
Epilepsy Unit Division of Cardiovascular & Medical Sciences, Western Infirmary, Glasgow G11 6NT, Scotland.
Curr Opin Pharmacol. 2006 Feb;6(1):108-13. doi: 10.1016/j.coph.2005.11.003. Epub 2005 Dec 22.
Gabapentin and pregabalin are structurally related compounds with recognized efficacy in the treatment of both epilepsy and neuropathic pain. The pharmacological mechanisms by which these agents exert their clinical effects have, until recently, remained unclear. The interaction of gabapentin and pregabalin with conventional antiepileptic and analgesic drug targets is likely to be modest, at best, and has been largely dismissed in favour of a selective inhibitory effect on voltage-gated calcium channels containing the alpha2delta-1 subunit. This mechanism is consistently observed in both rodent- and human-based experimental paradigms and may be sufficiently robust to account for much of the clinical activity of these compounds.
加巴喷丁和普瑞巴林是结构相关的化合物，在治疗癫痫和神经性疼痛方面具有公认的疗效。直到最近，这些药物发挥临床作用的药理机制仍不清楚。加巴喷丁和普瑞巴林与传统抗癫痫和镇痛药靶点的相互作用充其量可能很微弱，并且很大程度上已被摒弃，转而支持对含有α2δ-1亚基的电压门控钙通道具有选择性抑制作用。在基于啮齿动物和人类的实验范式中均一致观察到这种机制，并且可能足够强大，足以解释这些化合物的大部分临床活性。
