[Retention of metabolites of a beta-blocking drug, oxprenolol, in renal insufficiency].
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.
D001711:Biotransformation; D004305:Dose-Response Relationship, Drug; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007676:Kidney Failure, Chronic / Q000097:blood*; D008657:Metabolic Clearance Rate; D010096:Oxprenolol / Q000097:blood*; D006435:Renal Dialysis
D010096:Oxprenolol
Rétention des métabolites d'un médicament beta-bloquant, l'oxprénolol en cas d'insuffisance rénale.