Selectivity of bevantolol hydrochloride, a beta 1-adrenoceptor antagonist, in asthmatic patients.
Bevantolol hydrochloride, a new beta-adrenoceptor antagonist, has been shown to be cardioselective in animals. To evaluate its selectivity in humans, a double-blind, crossover study was conducted in 8 asthmatics. Following a single oral dose of placebo, bevantolol 75 or 150 mg or propranolol hydrochloride 40 mg, forced expiratory volume in 1 second (FEV1), heart rate, blood pressure and skeletal muscle tremor were measured before and after 4 increasing intravenous doses of terbutaline sulfate to establish terbutaline dose-response curves. The FEV1 decreased after all active treatments. During terbutaline infusions there was an increase in FEV1 after both bevantolol doses and placebo. The terbutaline dose-response curve after bevantolol shifted to the right, however. After propranolol, there was no increase in FEV1 during terbutaline stimulation. Heart rate and skeletal muscle tremor showed a similar pattern during the experiment. In dosages that have previously been shown to produce at least the same degree of blockade of exercise-induced tachycardia, bevantolol has less influence on terbutaline-induced bronchodilation, heart rate increase and skeletal muscle tremor than did propranolol. Thus bevantolol has relative beta 1-adrenoceptor antagonist selectivity. Drawing upon the results of a previous study in the same patients, we believe bevantolol, atenolol and metoprolol have similar beta 1-selectivity.
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology* / Q000627:therapeutic use; D000328:Adult; D000368:Aged; D001249:Asthma / Q000188:drug therapy*; D001794:Blood Pressure / Q000187:drug effects; D001980:Bronchi / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D005260:Female; D005541:Forced Expiratory Volume; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D008297:Male; D008875:Middle Aged; D009132:Muscles / Q000187:drug effects; D011412:Propanolamines / Q000494:pharmacology* / Q000627:therapeutic use; D011433:Propranolol / Q000494:pharmacology; D011897:Random Allocation
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; C021148:bevantolol; D011433:Propranolol