Role of cardioselectivity and intrinsic sympathomimetic activity in beta-blocking drugs in cardiovascular disease.
The significance of ancillary properties of beta blockers continues to be the focus of considerable clinical investigation. Beta 1-selective blocking agents, such as acebutolol, inhibit cardiac beta 1 receptors, but have less influence on bronchial and vascular beta 2 receptors. Certain beta 1-selective blocking drugs, including acebutolol, have intrinsic sympathomimetic activity (ISA), also termed partial agonist activity. This property produces slight cardiac stimulation, which can be blocked by propranolol. Drugs with mild or moderate ISA have proven to be as clinically effective as beta blockers lacking this property. Additionally, drugs with ISA possess potential therapeutic benefits, particularly for patients with coronary artery disease. The hemodynamic influences of cardioselectivity and ISA on left ventricular function, heart rate, cardiac output, left-sided heart filling pressure and myocardial oxygen consumption in patients with coronary artery disease are now clearly defined.
D000319:Adrenergic beta-Antagonists / Q000627:therapeutic use*; D000818:Animals; D002302:Cardiac Output / Q000187:drug effects; D002318:Cardiovascular Diseases / Q000188:drug therapy* / Q000503:physiopathology; D003326:Coronary Circulation / Q000187:drug effects; D004305:Dose-Response Relationship, Drug; D006321:Heart / Q000187:drug effects* / Q000503:physiopathology; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D009203:Myocardial Infarction / Q000188:drug therapy; D009928:Organ Specificity; D005082:Physical Exertion; D012146:Rest; D013566:Sympathomimetics / Q000627:therapeutic use*
D000319:Adrenergic beta-Antagonists; D013566:Sympathomimetics