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特罗地林在老年患者中的单剂量和多剂量药代动力学

Single- and multiple-dose pharmacokinetics of terodiline in geriatric patients.

作者信息

Hallén B, Magnusson A, Bogentoft S, Ekelund P

机构信息

Pharmacological Department, Kabi Vitrum AB, Stockholm, Sweden.

出版信息

Eur J Clin Pharmacol. 1988;34(3):291-7. doi: 10.1007/BF00540958.

Abstract

As a target group, geriataric patients were selected for pharmacokinetic studies with terodiline (Mictrol), an anticholinergic and calcium antagonist drug effective in the treatment of urinary incontinence. The single-dose kinetics in the geriatric patients (mean age 82 years) differed significantly from that previously found (Hallén et al. 1987) in healthy volunteers (mean age 35 years). There were higher peak serum concentrations (110 vs 79 micrograms.l-1), increased half-life (189 vs 60 h), lower renal clearance (4.0 vs 10.9 ml.min-1) and lower total clearance (29 vs 75 ml.min-1). Multiple-doses of 12.5 mg b.d. for 6-8 weeks resulted in a mean steady-state concentration of 642 micrograms.l-1, which was in agreement with the single dose parameters. The studied geriatric patients can be characterized not only as old, but also as frail, bedridden, having several diseases and polymedicated. The differences in pharmacokinetics between younger and elderly subjects can be attributed to a variety of complex factors, which may alter the clearance and/or the volume of distribution.

摘要

作为一个目标群体,老年患者被选来进行对特罗地林(Mictrol)的药代动力学研究,特罗地林是一种抗胆碱能和钙拮抗剂药物,对治疗尿失禁有效。老年患者(平均年龄82岁)的单剂量动力学与先前在健康志愿者(平均年龄35岁)中发现的情况(Hallén等人,1987年)有显著差异。血清峰值浓度更高(分别为110和79微克·升-1),半衰期延长(分别为189和60小时),肾脏清除率降低(分别为4.0和10.9毫升·分钟-1),总清除率降低(分别为29和75毫升·分钟-1)。每日两次服用12.5毫克,持续6至8周,导致平均稳态浓度为642微克·升-1,这与单剂量参数一致。所研究的老年患者不仅年老,而且体弱、卧床不起、患有多种疾病且用药种类多。年轻和老年受试者之间药代动力学的差异可归因于多种复杂因素,这些因素可能会改变清除率和/或分布容积。

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