Chemistry, physiology, and pharmacology of β-adrenergic mechanisms in the heart. Why are β-blocker antiarrhythmics superior?

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 Ca(2+) handling, are reviewed in this paper together with the clinical relevance of cardioprotective β-blocking therapy.

journal_name

Curr Pharm Des

authors

Szentmiklosi AJ,Szentandrássy N,Hegyi B,Horvath B,Magyar J,Bányász T,Nanasi PP

doi

10.2174/1381612820666141029111240

subject

Has Abstract

pub_date

2015-01-01 00:00:00

pages

1030-41

issue

8

eissn

1381-6128

issn

1873-4286

pii

CPD-EPUB-63125

journal_volume

21

pub_type

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