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[替仑西平在代偿期肝硬化患者中的药代动力学及耐受性]

[Pharmacokinetics and tolerability of telenzepine in patients with compensated liver cirrhosis].

作者信息

Reinicke A, Müller P, Dammann H G, Simon B

机构信息

Krankenhaus Schwetzingen, Medizinische Universitätsklinik Heidelberg.

出版信息

Arzneimittelforschung. 1990 Nov;40(11):1239-41.

PMID:2085337
Abstract

Pharmacokinetics and Tolerability of Telenzepine in Patients with Chronic Liver Diseases. The pharmacokinetics and tolerability of the new selective muscarinic M1-antagonist telenzepine (BY 803; CAS 80880-90-6) were studied in 10 patients with compensated liver cirrhosis who were treated over 4 weeks with 3 mg at night. 3 mg telenzepine was well tolerated. There was no deterioration of laboratory parameters during the 4 weeks treatment course. Following a single oral dose of 3 mg telenzepine the mean maximal plasma level (cmax) averaged 5.7 (1.9-10.1) ng/ml. After repeated dosing 3 patients displayed different kinetic behaviour resulting in higher values of AUC on day 14/15 in comparison to day 1/2. tmax and cmax remained unchanged. It can be concluded that even in patients with compensated liver cirrhosis no significant accumulation of the compound will occur.

摘要

替仑西平在慢性肝病患者中的药代动力学及耐受性。在10例代偿期肝硬化患者中研究了新型选择性毒蕈碱M1拮抗剂替仑西平(BY 803;化学物质登记号80880 - 90 - 6)的药代动力学及耐受性,这些患者在4周内每晚服用3毫克。3毫克替仑西平耐受性良好。在4周治疗过程中实验室参数无恶化。单次口服3毫克替仑西平后,平均最大血浆浓度(Cmax)平均为5.7(1.9 - 10.1)纳克/毫升。重复给药后,3例患者表现出不同的动力学行为,与第1/2天相比,第14/15天的曲线下面积(AUC)值更高。达峰时间(tmax)和最大血浆浓度(Cmax)保持不变。可以得出结论,即使在代偿期肝硬化患者中,该化合物也不会发生明显蓄积。

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