fesoterodine的药动学特征。

文章的细节

引用

复制到剪贴板

Malhotra B,关Z,木头N, Gandelman K

fesoterodine的药动学特征。

Int中国新药杂志。2008年11月,46 (11):556 - 63。

PubMed ID

19000553 (在PubMed

]

文摘

目的:Fesoterodine是一个新的antimuscarinic代理治疗膀胱过动症。口服后,fesoterodine迅速和广泛被非特异性酯酶水解其活跃的一部分:5-hydroxymethyl tolterodine (5-HMT)。细胞色素P450 (CYP)酶是没有参与5-HMT的形成;然而,CYP2D6和CYP3A4提供2 5-HMT的替代途径进一步代谢和失活。材料:单一口服剂量的4毫克,8毫克或12毫克的fesoterodine缓释片剂在禁食状态和8毫克美联储状态。方法:单中心,非盲、随机、交叉研究调查的影响fesoterodine CYP2D6在健康的志愿者组成的广泛的代谢(EMs);CYP2D6 n = 16)和贫穷的代谢(经前综合症;n = 8)在一夜之间迅速或高脂肪和高热量的早餐。不良事件、生命体征、心电图记录和实验室测试监控安全评估。结果:主要活动的一部分,5-HMT,最大血浆浓度(Cmax)曲线下的面积从0到时间的尿液中可测量的浓度(AUC0-t)和数量(Ae)按比例增加剂量EM和下午科目。 The mean Cmax and AUC0-t in PMs were approximately twice those observed in EMs. CYP2D6 status had no effect on time to reach Cmax (5 h), renal clearance (approximately 250 ml/min), or half-life (approximately 8 h). Fesoterodine was well tolerated at all doses. While the incidence of dry mouth increased from 8 - 12 mg, all occurrences were mild-to-moderate. CONCLUSIONS: Fesoterodine demonstrated a pharmacokinetic (PK) profile that was favorable for once-daily dosing. The systemic exposure to 5-HMT increased proportionally with dose and was about 2-fold higher in PMs compared with EMs. There was no clinically relevant effect of food on the PK of fesoterodine. Fesoterodine was well tolerated at all dose levels studied.

beplay体育安全吗DrugBank数据引用了这篇文章

药物酶

药物	酶	类	生物	药理作用	行动
Fesoterodine	细胞色素P450 2 d6	蛋白质	人类	未知的	底物	细节
Fesoterodine	细胞色素P450 3 a4	蛋白质	人类	未知的	底物	细节