Premium
The clinical pharmacology of bopindolol, a new long‐acting beta‐adrenoceptor antagonist, in hypertension
Author(s) -
Meiracker Anton H,
Man in 't Veld Arie J,
Ritsema van Eck Henk J,
Boomsma Frans,
Derkx Frans H M,
Mulder Paul,
Schalekamp Maarten A D H
Publication year - 1987
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1987.171
Subject(s) - medicine , blood pressure , heart rate , mean arterial pressure , vascular resistance , hemodynamics , cardiac output , partial agonist , placebo , clinical pharmacology , antagonist , anesthesia , cardiology , pharmacology , receptor , alternative medicine , pathology
Bopindolol is a new long‐acting, nonselective β‐adrenoceptor antagonist with partial agonist activity. Its acute (24 hours, 2 mg, administered orally) and long‐term (3 weeks, 2 to 4 mg) hemodynamic and hormonal effects were studied in a single‐blind placebo‐controlled trial in 10 hypertensive subjects. The initial response (mean ± SE) to bopindolol was a fall in cardiac output (−12% ± 2%) and heart rate (−11% ± 2%). Mean arterial pressure began to fall 3 to 4 hours after administration in parallel with a decrease in systemic vascular resistance, which had increased initially. Twenty‐four hours after administration, mean arterial pressure and systemic vascular resistance were reduced by 12% ± 2% and 12% ± 5%, respectively. By that time heart rate and cardiac output did not differ from baseline values despite β‐blockade. After 3 weeks of treatment mean arterial pressure had fallen by 9% ± 2% and renal blood flow and glomerular filtration rate were not changed. One week after withdrawal from treatment mean arterial pressure and heart rate were no longer reduced, but β‐blockade could still be demonstrated, establishing the long duration of action of the drug. Clinical Pharmacology and Therapeutics (1987) 42, 411–419; doi: 10.1038/clpt.1987.171