Chemistry, Physiology, and Pharmacology of β-Adrenergic Mechanisms in the Heart. Why are β-Blocker Antiarrhythmics Superior?

Title:Chemistry, Physiology, and Pharmacology of β-Adrenergic Mechanisms in the Heart. Why are β-Blocker Antiarrhythmics Superior?

Volume: 21 Issue: 8

Author(s): A. Jozsef Szentmiklosi, Norbert Szentandrassy, Bence Hegyi, Balazs Horvath, Janos Magyar, Tamas Banyasz and Peter P. Nanasi

Affiliation:

Keywords: β-adrenergic receptors, β-receptor blockers, proarrhythmic mechanisms, antiarrhythmic drugs, cardiac ion currents, cardiac remodeling.

Abstract: Stimulation of β-adrenergic receptors in the heart is the most effective endogenous way to increase the mechanical performance of cardiac tissues to meet the requirements of a fight-or-flight situation or stress. On the other hand, sustained activation of cardiac β-receptors initiates maladaptive remodeling of the myocardium leading to cardiomyopathies and heart failure. Since both acute and chronic stimulation of β-adrenoceptors are arrhythmogenic, the application of β-receptor blockers exerts effective antiarrhytmic actions at both short and long time scale. Compared to other classes of antiarrhythmic agents, β-blockers are the class of antiarrhythmics that was shown to decrease mortality in postinfarct patients. Chemical, physiological, and pharmacological properties of the β-adrenoceptor related signaling, the role of β-1, β-2, and β-3 receptor subtypes, consequences of acute and long term β-adrenergic stimulation and the underlying proarrhythmic mechanisms, including the changes in cardiac ion currents and Ca²⁺ handling, are reviewed in this paper together with the clinical relevance of cardioprotective β-blocking therapy.

Cite this article as:

Szentmiklosi Jozsef A., Szentandrassy Norbert, Hegyi Bence, Horvath Balazs, Magyar Janos, Banyasz Tamas and Nanasi P. Peter, Chemistry, Physiology, and Pharmacology of β-Adrenergic Mechanisms in the Heart. Why are β-Blocker Antiarrhythmics Superior?, Current Pharmaceutical Design 2015; 21 (8) . https://dx.doi.org/10.2174/1381612820666141029111240