Clinical pharmacology of a new beta-adrenoceptor blocking drug, befunolol. Cross-over comparison with propranolol on repeated administration.
Repeated doses of a new beta-adrenoceptor blocking agent, befunolol, were administered orally to adult male volunteers for a cross-over comparison with propranolol. The beta-adrenoceptor blocking activity of befunolol was greater than that of propranolol when assessed by the percentage reduction in exercise-induced tachycardia. The elimination half-life of drug was significantly prolonged on repeated administration of propranolol, but not of befunolol. The percentage reduction in exercise-induced tachycardia was highly correlated with the log plasma level of each drug. Both drugs produced a significant reduction in pre-exercise systolic and diastolic blood pressure, and significant attenuation of exercise-induced rise in systolic blood pressure.
D000319:Adrenergic beta-Antagonists / Q000008:administration & dosage / Q000097:blood / Q000494:pharmacology*; D000328:Adult; D001794:Blood Pressure / Q000187:drug effects; D005080:Exercise Test; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D007700:Kinetics; D008297:Male; D005082:Physical Exertion / Q000187:drug effects; D011412:Propanolamines / Q000008:administration & dosage / Q000097:blood / Q000494:pharmacology*; D011433:Propranolol / Q000008:administration & dosage / Q000097:blood / Q000494:pharmacology*
D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; C006034:befunolol; D011433:Propranolol