title: A comparison of single doses of bucindolol and oxprenolol in hypertensive patients.
abstract: Single doses of bucindolol 50, 100 and 200 mg were compared to placebo and single doses of oxprenolol 40, 80 and 160 mg in seven patients with mild hypertension, in a double-blind randomized study. Both bucindolol and oxprenolol inhibited exercise induced tachycardia. The mean maximum inhibition of exercise heart rate was similar after each dose of both drugs (20%, P less than 0.001). Bucindolol produced a significantly greater reduction in blood pressure than either oxprenolol or placebo. This was most apparent in standing systolic and diastolic and post-exercise systolic blood pressures between 1 and 2 h after dosing and was dose-related. All seven patients experienced adverse effects related to hypotension within the first 2 h after ingestion of bucindolol 200 mg. Plasma concentrations of oxprenolol, bucindolol or 5-hydroxy-bucindolol, sampled 2 h after dosing, could not be related to either the changes in blood pressure or to the occurrence of symptoms. The results emphasise the need for careful dose-finding of new drugs prior to their more widespread evaluation in phase 3 studies.
authors.forename: J
authors.initials: J
authors.lastname: Webster
authors.forename: J C
authors.initials: JC
authors.lastname: Petrie
authors.forename: O J
authors.initials: OJ
authors.lastname: Robb
authors.forename: M
authors.initials: M
authors.lastname: Jamieson
authors.forename: J
authors.initials: J
authors.lastname: Verschueren
mesh_terms: D000319:Adrenergic beta-Antagonists / Q000009:adverse effects / Q000097:blood / Q000627:therapeutic use*; D000328:Adult; D001794:Blood Pressure / Q000187:drug effects; D005080:Exercise Test; D005260:Female; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000503:physiopathology; D008297:Male; D008875:Middle Aged; D010096:Oxprenolol / Q000009:adverse effects / Q000097:blood / Q000627:therapeutic use*; D011187:Posture; D011412:Propanolamines / Q000009:adverse effects / Q000097:blood / Q000627:therapeutic use*; D013997:Time Factors
chemical_list: D000319:Adrenergic beta-Antagonists; D011412:Propanolamines; D010096:Oxprenolol; C024307:bucindolol