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Molecules 2012, 17(11), 13592-13604; doi:10.3390/molecules171113592

Ivabradine: An Intelligent Drug for the Treatment of Ischemic Heart Disease

Intensive Cardiology Care Unit, San Camillo de Lellis Hospital, Manfredonia, via Isonzo, 71043 Foggia, Italy
Received: 10 October 2012 / Revised: 30 October 2012 / Accepted: 30 October 2012 / Published: 16 November 2012
(This article belongs to the Special Issue Ivabradine)
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Abstract

Heart rate (HR) is a precisely regulated variable, which plays a critical role in health and disease. Elevated resting HR is a significant predictor of all-cause and cardiovascular mortality in the general population and patients with cardiovascular disease (CVD). β-blocking drugs exert negative effects on regional myocardial blood flow and function when HR reduction is eliminated by atrial pacing; calcium channel antagonists (CCAs) functionally antagonize coronary vasoconstriction mediated through α-adreno-receptors and are thus devoid of this undesired effect, but the compounds are nevertheless negative inotropes. From these observations derives the necessity to find alternative, more selective drugs to reduce HR through inhibition of specific electrical current (If). Ivabradine (IVA) is a novel specific HR-lowering agent that acts in sinus atrial node (SAN) cells by selectively inhibiting the pacemaker If current in a dose-dependent manner by slowing the diastolic depolarization slope of SAN cells, and by reducing HR at rest during exercise in humans. Coronary artery diseases (CAD) represent the most common cause of death in middle–aged and older adults in European Countries. Most ischemic episodes are triggered by an increase in HR, that induces an imbalance between myocardial oxygen delivery and consumption. IVA, a selective and specific inhibitor of the If current which reduced HR without adverse hemodynamic effects, has clearly and unequivocally demonstrated its efficacy in the treatment of chronic stable angina pectoris (CSAP) and myocardial ischemia with optimal tolerability profile due to selective interaction with If channels. The aim of this review is to point out the usefulness of IVA in the treatment of ischemic heart disease.
Keywords: angina; coronary artery disease; fanny current; HCN channels; heart rate; ivabradine; sino atrial node angina; coronary artery disease; fanny current; HCN channels; heart rate; ivabradine; sino atrial node
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Riccioni, G. Ivabradine: An Intelligent Drug for the Treatment of Ischemic Heart Disease. Molecules 2012, 17, 13592-13604.

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