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ß-Adrenergic Blockers as Antiarrhythmic and Antifibrillatory Compounds: An Overview

Department of Cardiology, VA Medical Center, West Los Angeles, and Department of Medicine, David Geffen School of Medicine at UCLA, Los Angeles, CA

ß-Adrenergic blockers have a wide spectrum of action for controlling cardiac arrhythmias that is larger than initially thought. Data from the past several decades indicate that, as an antiarrhythmic class, ß-blockers remain among the very few pharmacologic agents that reduce the incidence of sudden cardiac death, prolong survival, and ameliorate symptoms caused by arrhythmias in patients with cardiac disease. As a class of compounds, ß-blockers have a fundamental pharmacologic property that attenuates the effects of competitive adrenergic receptors. However, the net clinical effects of the different ß-receptor blockers may vary quantitatively because of variations in associated intrinsic sympathomimetic agonism and in their intrinsic potency for binding to ß-receptors. These individual compounds also differ in their selectivity for ß₁- and ß₂-receptors. Metoprolol is a ß₁-selective blocker, whereas carvedilol is a nonselective ß₁- and ß₂-blocker, an antioxidant, and has a propensity to inhibit ₁-receptors and endothelin. Evolving data from controlled and uncontrolled clinical trials suggest that there are clinically significant differences among this class of drugs. Recent evidence also suggests that the antiarrhythmic actions of certain ß-receptor blockers such as carvedilol and metoprolol extend beyond the ventricular tissue to encompass atrial cells and help maintain sinus rhythm in patients with atrial fibrillation, especially in combination with potent antifibrillatory agents such as amiodarone. This introduction provides a current perspective on these newer developments in the understanding of the antiarrhythmic and antifibrillatory actions of ß-blockers.

Key Words: ß-blockers • antiarrhythmics • selective versus nonselective ß-blockers • atrial fibrillation • carvedilol • metoprolol

Journal of Cardiovascular Pharmacology and Therapeutics, Vol. 10, No. 4 suppl, S3-S14 (2005)
DOI: 10.1177/10742484050100i402


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