Koopmans R, Oosterhuis B, Karemaker J M, Wemer J, van Boxtel C J
Department of Medicine, University of Amsterdam, The Netherlands.
Eur J Clin Pharmacol. 1988;34(4):395-400. doi: 10.1007/BF00542442.
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.
在6名健康志愿者中研究了氧烯洛尔血浆浓度与其在体育锻炼期间血流动力学效应之间的关系。在治疗后8小时内，通过重复三分钟的运动期，使用无创技术（Fin-A-Press血压计）连续监测他们的血压和心率（HR）。使用拟合的药代动力学曲线，采用Emax模型将药物效应与其血浆浓度相关联。运动期间药物浓度与心率（HRex）之间关系的平均EC50为73.1 ng/ml，运动期间收缩压（SBPex）的平均EC50为112.7 ng/ml。HRex的Emax为29.0%，SBPex的Emax为33.2%。对HRex和SPBex影响的参数之间没有一致的差异。因此，使用一种新的无创技术连续测量血压，β-肾上腺素受体阻断药物对SBPex的影响与对HRex的影响描述精度相似。
