Amlodipine

Amlodipine is a long-acting calcium channel blocker.Target: Calcium ChannelAmlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the movement of calcium ions into vascular smooth muscle cells and cardiac muscle cells. Experimental data suggest amlodipine binds to both dihydropyridine and nondihydropyridine binding sites. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of ext
Amlodipine is a dihydropyridine L-type calcium channel blocker that selectively inhibits calcium influx in cardiac and vascular smooth muscle. Acting as a vasodilator, amlodipine reduces blood pressure by relaxing the smooth muscle in the arterial wall, decreasing total peripheral resistance. It inhibits calcium-induced contractions in depolarized rat aorta with an IC50value of 1.9 nM, displaying a slow rate of association and dissociation in isolated vascular and cardiac tissues. Amlodipine also demonstrates actions independent of L-type calcium channel blockade by regulating membrane fluidity and cholesterol deposition, stimulating nitric oxide production, acting as an antioxidant, and regulating matrix depositionin vitroandin vivo. Formulations containing amlodipine have been used in the treatment of hypertension.
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Amlodipine was first patented in 1982 but approved as a prescription drug in 1990. Amlodipine is in the form of salt, the available salt forms are besilat, mesilate, and maleate. Amlodipine is an approved drug used to treat high blood pressure and coronary artery disease. Amlodipine is also sold under the brand name Norvasc. It was evaluated against diuretics in the treatment of hypertension and was found to be useful in controlling arterial pressure. In 2023, it was the fifth most commonly prescribed medication in the United States, with more than 68 million prescriptions.
ChEBI: A fully substituted dialkyl 1,4-dihydropyridine-3,5-dicarboxylate derivative, which is used for the treatment of hypertension, chronic stable angina and confirmed or suspected vasospastic angina.