Mechanism action of Bepridil
Bepridil has inhibitory effects on both the slow calcium (L-type) and
fast sodium inward currents in myocardial and vascular smooth muscle,
interferes with calcium binding to calmodulin, and blocks both voltage
and receptor operated calcium channels. Bepridil inhibits the
transmembrane influx of calcium ions into cardiac and vascular smooth
muscle. This has been demonstrated in isolated myocardial and vascular
smooth muscle preparations in which both the slope of the calcium dose
response curve and the maximum calcium-induced inotropic response were
significantly reduced by bepridil. In cardiac myocytes in vitro,
bepridil was shown to be tightly bound to actin. Bepridil regularly
reduces heart rate and arterial pressure at rest and at a given level of
exercise by dilating peripheral arterioles and reducing total
peripheral resistance (afterload) against which the heart works.
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