Pharmacokinetic-pharmacodynamic modelling of oxprenolol in man using continuous non-invasive blood pressure monitoring |
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| Authors: | R. Koopmans B. Oosterhuis J. M. Karemaker J. Wemer C. J. van Boxtel |
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| Affiliation: | (1) Clinical Pharmacology section, Departments of Medicine and Pharmacology, University of Amsterdam, Amsterdam, The Netherlands;(2) Department of Physiology, Academic Medical Center, University of Amsterdam, Amsterdam, The Netherlands |
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| Abstract: | Summary The relationship between the plasma concentration of oxprenolol and its haemodynamic effects during physical exercise was studied in 6 healthy volunteers, in whom BP and heart rate (HR) were continuously monitored by non-invasive techniques (Fin-A-Press-Tonometer) during repeated three-minute exercise periods for 8 h after treatment. Using the fitted pharmacokinetic curve, the drug effect was related to its plasma concentration using the Emax model.The mean EC50 for the relationship between drug concentration and heart rate during exercise (HRex) was 73.1 ng/ml, and for systolic blood pressure during exercise (SBPex) it was 112.7 ng/ml. Emax was 29.0% for HRex, and 33.2% for SBPex. There were no consistent differences between the parameters for the effects on HRex and SPBex.Thus, using a new, non-invasive technique for continuous measurement of blood pressure, the effect of a beta-adrenoceptor blocking drug on SBPex was described with similar accuracy as its effect on HRex. |
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| Keywords: | oxprenolol beta-blockade concentration-effect relationship non-invasive monitoring exercise test blood pressure monitoring healthy volunteers predictive model |
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