Ding R W, Port R E, Ortmann K, Liebmann B, Spahn-Langguth H, Mutschler E, Weber E
Department of Clinical Pharmacology, University Medical Centre, Heidelberg, Germany.
Eur J Clin Pharmacol. 1994;46(5):455-9. doi: 10.1007/BF00191911.
Ciclotropium is a recently developed parasympathicolytic agent. Plasma concentration and heart rate increase (the most prominent anticholinergic effects) were measured in 12 healthy subjects before, during and after a 15-min intravenous infusion of 10 mg ciclotropium. The effect was described by using either a linear or a nonlinear (Emax) effect model linked to a linear three-compartment kinetic model via an effect compartment. Maximum heart rate increase was 33 (10) beats.min-1, and half-value duration of effect was 41 (9) min. Total plasma clearance was 0.51 (0.13) l.min-1, and mean terminal elimination half-life was 12(4) h, whereas the equilibration half-lives of drug removal from the effect compartment ranged from 2 to 14 min.
噻托溴铵是一种最近研发的抗胆碱能药物。在12名健康受试者中，于静脉输注10毫克噻托溴铵15分钟之前、期间和之后，测量了血浆浓度和心率增加情况（最显著的抗胆碱能效应）。通过使用线性或非线性（Emax）效应模型来描述该效应，这些模型通过一个效应室与线性三室动力学模型相联系。最大心率增加为33（10）次·分钟⁻¹，效应的半衰期为41（9）分钟。血浆总清除率为0.51（0.13）升·分钟⁻¹，平均终末消除半衰期为12（4）小时，而药物从效应室消除的平衡半衰期为2至14分钟。
