Description
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).
.
Chemical Properties
White to Off-White Solid
Originator
Servier (France)
Uses
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
Uses
Selective bradycardic agent with direct effect on the pacemaker If current of the sinoatrial node. Antianginal
Uses
Ivabradine hydrochloride has been used as a potassium/sodium hyperpolarization-activated cyclic nucleotide-gated channel (HCN)2 blocker in embryoid body (EB) and rat engineered heart tissue (EHT).
Definition
ChEBI: A hydrochloride obtained by combining ivabradine with one molar equivalent of hydrochloric acid. Used to treat patients with angina who have intolerance to beta blockers and/or heart failure.
Biochem/physiol Actions
Ivabradine is used to treat chronic heart failure.
Clinical Use
Symptomatic treatment of chronic stable angina pectoris
in patients with sinus rhythm
Treatment of mild to severe chronic heart failure
