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 (E max) 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.
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Ding, R.W., Port, R.E., Ortmann, K. et al. The effect of ciclotropium on human heart rate. Eur J Clin Pharmacol 46, 455–459 (1994). https://doi.org/10.1007/BF00191911
- heart rate
- pharmacokinetic/pharmacodynamic modelling
- effect compartment