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美哌洛尔经皮给药的人体药理学研究。药效学与定向药代动力学

[Human pharmacologic studies on transdermal administration of mepindolol. Pharmacodynamic and orienting pharmacokinetics].

作者信息

Liedtke R K, Chen L S, Mangold B, Haase W

机构信息

Wissenschaftliche Abteilung der pharmed GmbH, Universität Würzburg.

出版信息

Arzneimittelforschung. 1989 Nov;39(11A):1501-4.

PMID:2576199
Abstract

The pharmacodynamic effects of acute and repeated application of a transdermal patch (BIO TSD) containing 20 mg of the beta-receptor blocking agent mepindolol were assessed in 13 normotensive male volunteers. Orienting measurements of mepindolol serum levels were performed additionally. At rest, the effects on blood pressure and heart rate were very limited. However, during submaximum ergometer exercise, significant systemic beta-blocking effects were observed, especially after 5 days treatment. Repeated administration did not induce tachyphylaxis but resulted in an enhanced efficacy. The mepindolol serum concentrations were markedly lower than those measured after oral application of the drug. No systemic or local adverse reactions nor any relevant changes in laboratory parameters were observed.

摘要

在13名血压正常的男性志愿者中评估了含有20毫克β受体阻滞剂美吲哚洛尔的透皮贴剂(BIO TSD)急性和重复应用的药效学效应。另外还进行了美吲哚洛尔血清水平的定向测量。静息时,对血压和心率的影响非常有限。然而,在次极量测力计运动期间,观察到显著的全身性β受体阻滞作用,尤其是在治疗5天后。重复给药未引起快速耐受性,反而导致疗效增强。美吲哚洛尔血清浓度明显低于口服该药后测得的浓度。未观察到全身性或局部不良反应,实验室参数也未出现任何相关变化。

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