Description
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In an effort to develop angina agents without the unwanted negative inotropic and hypotensive effects associated with b-adrenergic blockers and calcium channel blockers, a new class of heart-rate reducing compounds that act specifically on the sinoatrial (SA) node has been explored. These bradycardic agents interact directly with the pacemaking cell of the SA node and the hyperpolarization- activated If , the primary pacemaking current. Ivabradine has evolved as a specific inhibitor of If current through its contact with f-channels on the intracellular side of the plasma membrane. As a consequence, ivabradine reduces the speed of diastolic depolarization and decreases heart rate. It has been approved for the treatment of chronic stable angina and provides a viable alternative to patients with a contraindication or intolerance of b-blockers. Evaluation is also underway for the potential treatment of ischemic heart disease. Using a patch-clamp technique on rabbit sinoatrial node cells, inhibition of If current ranged from 6% (0.03 mM) - 80% (10 mM). .
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Chemical Properties
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White to Off-White Solid
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Originator
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Servier (France)
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Uses
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Selective bradycardic agent with direct effect on the pacemaker If current of the sinoatrial node. Antianginal
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Uses
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Ivabradine HCl, a new If inhibitor with IC 50 of 2.9 μM which acts specifically on the pacemaker activity of the sinoatrial node, is a pure heart rate lowering agent
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Uses
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angina therapeutic
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Definition
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ChEBI: A hydrochloride obtained by combining ivabradine with one molar equivalent of hydroc hloric acid. Used to treat patients with angina who have intolerance to beta blockers and/or heart failure.
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Brand name
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Procoralan
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