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).
.
화학적 성질
White to Off-White Solid
용도
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).
정의
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.
