年龄和性别对retigabine处置。

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赫尔曼·R,铁试剂通用,Erb K, Knebel N, ruu刷机程序P,保罗J,理查兹L, Cnota惠普,特洛伊

年龄和性别对retigabine处置。

中国新药杂志。2003年1月,73 (1):61 - 70。

PubMed ID

12545144 (在PubMed

]

文摘

背景:新型抗癫痫药物retigabine是第一个选择性M-current钾通道揭幕战KCNQ2/3和KCNQ3/5频道。Retigabine经历二期新陈代谢(N-glucuronidation,乙酰化)专门和肾排泄。目的:我们的目标是评估年龄和性别的影响retigabine的药物动力学。方法:健康的年轻(年龄范围,18-40年)和老年人(年龄范围,66 - 81年)白色受试者(男12女在每组12日)收到一个200毫克口服剂量的retigabine。剂量后,血液被收集在72小时内确定等离子体浓度retigabine及其乙酰化代谢物,awd21 - 360。药物动力学比较年龄和性别的方差分析。结果:在年轻人,retigabine迅速吸收,最大浓度在2小时内发生,消除了一个明显的间隙为0.67 L x h(1)公斤(1)和平均终端半衰期8.5小时。受试者同样暴露awd21 - 360。与年轻人相比,年轻女性有更高retigabine最大浓度(56%)和接触(20%),但类似的间隙(0.68 L x h(1)千克(1));这些差异是体重的差异。 Although maximum concentration was similar in elderly subjects, retigabine elimination was slower (30% lower apparent clearance normalized for weight), resulting in higher exposure (42%) and a longer half-life (30%). Because phase II metabolism is scarcely affected by age, these differences may be related to the known decline of renal function with age. CONCLUSIONS: Although there are no substantial sex-related differences in the disposition of retigabine, a relevant decrease in clearance resulting in higher exposure occurs in elderly patients. The results suggest that decline of renal function with age may account for some of the observed changes.

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药物

Ezogabine

药物靶点

药物	目标	类	生物	药理作用	行动
Ezogabine	电压门控钾通道亚KQT成员5	蛋白质	人类	未知的	不可用	细节