Brunner L, Imhof P, Jack D
Eur J Clin Pharmacol. 1975;8(1):3-9. doi: 10.1007/BF00616408.
Oxprenolol, 40, 80 and 160 mg, was administered orally to seven healthy volunteers. Over the following eight hours repeated measurements were made of the plasma concentrations and effects on heart rate, myocardial contractility (PEPc) and systolic and diastolic blood pressure in recumbency, in the upright position and during physical effort at a work load of 120 watts on a bicycle ergometer. The maximum plasma levels and the area beneath the plasma concentration curves increased roughly in proportion to the dosage increment. No evidence of first-pass inactivation in the liver was found. The half-life of the drug in plasma was approximately 80 minutes, irrespective of the dose administered. Oxprenolol slowed heart rate, prolonged PEPc and lowered systolic blood pressure, by comparison with values recorded after a placebo. The effects were generally least marked in the recumbent position and most marked during effort, when a clear-cut dose-response relation was found. The pharmacodynamic effects of oxprenolol were compared with its concentration in plasma. Marked beta-receptor blockade still persisted eight hours after dosing, although at this time, after doses of 40 and 80 mg, the drug could not be detected in plasma.
对7名健康志愿者口服氧烯洛尔，剂量分别为40毫克、80毫克和160毫克。在随后的8小时内，对他们在卧位、直立位以及在自行车测力计上以120瓦的工作负荷进行体力活动期间的血浆浓度以及心率、心肌收缩力（左室射血前期）和收缩压与舒张压的影响进行了重复测量。最大血浆浓度和血浆浓度曲线下面积大致随剂量增加而成比例增加。未发现该药物在肝脏存在首过灭活现象。无论给药剂量如何，该药物在血浆中的半衰期约为80分钟。与服用安慰剂后记录的值相比，氧烯洛尔可减慢心率、延长左室射血前期并降低收缩压。这些效应通常在卧位时最不明显，在体力活动期间最明显，此时可发现明确的剂量-反应关系。将氧烯洛尔的药效学效应与其血浆浓度进行了比较。给药8小时后，尽管此时在服用40毫克和80毫克剂量后血浆中已检测不到该药物，但仍存在明显的β受体阻滞作用。
