Comparative beta-adrenoceptor blocking effects and pharmacokinetics of penbutolol and propranolol in man.
1 The beta-adrenoceptor blocking effects of penbutolol were compared with those of propranolol and a placebo in a double-blind trial involving six healthy volunteers. 2 Heart rate (HR), systolic blood pressure (SBP) and peak expiratory flow rate (PEFR) were measured at rest and during vigorous exercise before and at intervals up to 7 h after oral administration of the drugs. In addition, plasma renin activity (PRA) at rest and plasma levels of penbutolol and propranolol were determined. 3 Penbutolol proved to be a non-cardioselective beta-adrenoceptor blocking drug, antagonizing exercise-induced tachycardia, reducing exercise-induced increase in PEFR and decreasing PRA. The beta-adrenolytic potency of penbutolol was shown to be four-fold that of propranolol but the duration of its effect was similar. 4 The peak plasma level of penbutolol was reached 1 h after administration and its half-life was 4.5 h. 5 Comparison of plasma levels and biological activity of penbutolol revealed that after oral administration this drug is transformed into an active metabolite in man.
D000319:Adrenergic beta-Antagonists; D000328:Adult; D001794:Blood Pressure / Q000187:drug effects; D002849:Chromatography, Gas; D003517:Cyclopentanes / Q000097:blood / Q000494:pharmacology; D004311:Double-Blind Method; D004361:Drug Tolerance; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007700:Kinetics; D008297:Male; D010366:Peak Expiratory Flow Rate; D011412:Propanolamines / Q000097:blood / Q000494:pharmacology*; D011433:Propranolol / Q000097:blood / Q000494:pharmacology*; D012083:Renin / Q000097:blood
D000319:Adrenergic beta-Antagonists; D003517:Cyclopentanes; D011412:Propanolamines; D011433:Propranolol; D012083:Renin