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Levoamlodipine besilate is the chirally pure (S)-enantiomer of the racemic calcium channel blocker amlodipine. It functions as a long-acting dihydropyridine calcium channel antagonist that selectively inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle cells by blocking L-type calcium channels. This inhibition leads to peripheral vasodilation and a reduction in total peripheral vascular resistance, thereby lowering blood pressure. As the active enantiomer, levoamlodipine provides comparable antihypertensive efficacy to racemic amlodipine at approximately half the dose, which may reduce the incidence of dose-dependent adverse effects such as peripheral edema. It is primarily indicated for the treatment of essential hypertension and chronic stable angina. In addition to its use as a monotherapy, it is being developed in fixed-dose combinations with other antihypertensive agents, such as bisoprolol fumarate.
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