Dayer P, Glasson P, Gorgia A, Balant L, Fabre J
Schweiz Med Wochenschr. 1981 Dec 5;111(49):1915-8.
The pharmacokinetics in blood of oxprenolol and its glucuro-conjugated metabolites has been investigated in healthy volunteers and hemodialyzed patients; in addition, the effect of the drug on the heart rate has been measured. Renal insufficiency does not modify the elimination kinetics of oxprenolol, but it does lead to massive retention of the glucuro-conjugated derivatives on multiple dosing. The present study failed to show hydrolysis of the conjugates with liberation of the active parent compound. In addition, from measurement of the exercise-stimulated heart rate it can be concluded that active metabolites of oxprenolol are absent. The duration and intensity of the effect of a single dose of the drug were comparable in the healthy volunteers and the patients with renal insufficiency.
已在健康志愿者和接受血液透析的患者中研究了氧烯洛尔及其葡萄糖醛酸结合代谢物在血液中的药代动力学；此外，还测量了该药物对心率的影响。肾功能不全不会改变氧烯洛尔的消除动力学，但多次给药时确实会导致葡萄糖醛酸结合衍生物的大量潴留。本研究未能显示结合物水解并释放出活性母体化合物。此外，通过测量运动刺激的心率可以得出结论，氧烯洛尔不存在活性代谢物。单剂量药物的作用持续时间和强度在健康志愿者和肾功能不全患者中相当。
