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

A. József Szentmiklósi, Norbert Szentandrássy, Bence Hegyi, Balázs Horváth, János Magyar, Tamás Bányász, Péter P. Nánási

Research output: Contribution to journalArticle

6 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)1030-1041
Number of pages12
JournalCurrent pharmaceutical design
Volume21
Issue number8
DOIs
Publication statusPublished - Jan 1 2015

Keywords

  • Antiarrhythmic drugs
  • B-adrenergic receptors
  • B-receptor blockers
  • Cardiac ion currents
  • Cardiac remodeling
  • Proarrhythmic mechanisms

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery

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