抗癫痫药物治疗特发性广泛性癫痫的性质。

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Patsalos PN

抗癫痫药物治疗特发性广泛性癫痫的性质。

癫痫病。2005;46增刊9:140-8。

PubMed ID

16302888 (PubMed视图

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摘要

虽然丙戊酸钠被认为是治疗特发性广泛性癫痫(IGEs)的首选药物，但其他抗癫痫药物(aed)，包括旧的(乙氧酰亚胺、氯巴坦和氯硝西泮)和新的(拉莫三嗪、左乙拉西坦、托吡酯和唑尼沙胺)也可用。这些aed似乎没有共同的作用机制，即抑制γ -氨基丁酸(GABA;例如，氯巴萨姆，氯硝西泮和丙戊酸盐)和兴奋性谷氨酸(例如，拉莫三嗪和托吡酯)机制涉及。乙磺酰亚胺主要通过阻断丘脑神经元的t型电压门控钙通道起作用，托吡酯和唑尼沙胺具有多种作用机制。相比之下，左乙拉西坦的独特之处在于它可能通过大脑中的特定结合位点起作用。就其药代动力学特征而言，所有8种aed口服后均可迅速吸收，并在1-4小时内达到血药浓度峰值。生物利用度为100%，氯硝西泮(90%)和托吡酯(81-95%)除外。血浆蛋白结合是可变的，丙戊酸钠(90%)，氯巴坦(85%)和氯硝西泮(86%)具有大量结合，拉莫三嗪(55%)和唑尼沙胺(50%)中间结合，左乙拉西坦(0%)，乙氧酰亚胺(0%)和托吡酯(10%)结合最少。然而，佐尼沙胺与红细胞和白蛋白的结合是复杂的。除拉莫三嗪和左乙拉西坦外，所有ads都因肝细胞色素P450酶的广泛代谢而被消除，这些酶对其他药物的诱导和抑制非常敏感，因此易受药代动力学相互作用的影响。 Lamotrigine metabolism is via hepatic glucuronidation, a process that is also susceptible to induction and inhibition by concurrent drugs. Levetiracetam is minimally metabolized (by hydrolysis in blood), is excreted predominantly unchanged in urine, and to date has not been associated with any clinically significant pharmacokinetic interactions. Using a semiquantitative pharmacokinetic rating system, based on 16 pharmacokinetic characteristics, a direct comparison between AEDs is possible. Thus valproic acid, regarded as the drug of first choice in the treatment of IGEs, rates lowest with respect to favorable pharmacokinetic characteristics, mostly because of its nonlinear pharmacokinetics, extensive hepatic metabolism, and its high propensity to interact both with other AEDs and non-AEDs. Levetiracetam rates highest with topiramate in second place.

引用本文的药物库数据

药物

乙琥胺