Small molecule
PubChem CID 2162
Amlodipine
Norvasc
- Mechanism of action
- L-type calcium channel blocker
- In plain language
- Relaxes and widens blood vessels by blocking calcium from entering their muscle cells, easing the heart's workload and lowering blood pressure.
- How it works
- Amlodipine is a dihydropyridine calcium channel blocker that binds L-type calcium channels on vascular smooth muscle and cardiac muscle, inhibiting transmembrane calcium ion influx. It acts with selectively greater potency on vascular smooth muscle than on cardiac muscle, so its dominant effect is peripheral arterial vasodilation, which reduces peripheral vascular resistance and lowers blood pressure. Its slow association/dissociation kinetics at the receptor binding site produce a gradual onset and prolonged, smooth duration of action, supporting once-daily dosing. In the coronary circulation, amlodipine also dilates coronary arteries and arterioles, increasing myocardial oxygen supply and counteracting coronary vasoconstriction, which relieves both exertional and vasospastic (Prinzmetal's) angina.
- Therapeutic applications
- Indicated for the treatment of hypertension, to lower blood pressure and reduce the risk of fatal and nonfatal cardiovascular events, primarily stroke and myocardial infarction (approved for adults and pediatric patients 6-17 years). Also indicated for coronary artery disease: chronic stable angina, vasospastic (Prinzmetal's/variant) angina, and angiographically documented coronary artery disease in patients without heart failure or an ejection fraction below 40%, to reduce the risk of hospitalization for angina and the need for revascularization procedures.
- Class
- Small molecule
- Therapeutic area
- Cardiovascular
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