Amlodipine

Amlodipine is a dihydropyridine calcium channel blocker (CCB) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. By blocking calcium entry into smooth muscle cells in blood vessel walls, amlodipine causes vasodilation — relaxation and widening of blood vessels — which reduces peripheral vascular resistance and lowers blood pressure. It also dilates coronary arteries, increasing coronary blood flow and reducing the oxygen demand of the heart muscle, which is the basis for its use in angina.¹

Amlodipine has a very long elimination half-life of approximately 30–50 hours, enabling once-daily dosing with gradual, stable blood pressure reduction and a low risk of sudden blood pressure drops.

Hypertension — to lower blood pressure. Lowering blood pressure reduces the risk of fatal and non-fatal cardiovascular events, primarily strokes and myocardial infarctions.

Coronary artery disease — chronic stable angina, vasospastic angina (Prinzmetal's or variant angina), and angiographically documented coronary artery disease to reduce the risk of hospitalization for angina and revascularization procedures.¹

For hypertension and angina: Starting dose is typically 5 mg once daily. May be increased to 10 mg once daily after 7–14 days if needed. Smaller patients, frail patients, and those with hepatic impairment may start at 2.5 mg once daily.¹

Oral tablets.

Store at controlled room temperature (59°F to 86°F / 15°C to 30°C).¹

Key considerations from the FDA label:¹

• Peripheral edema: The most common side effect — ankle and lower leg swelling occurs in approximately 10% of patients at 5 mg and more frequently at 10 mg. This is a direct result of the vasodilatory mechanism and is not a sign of heart or kidney disease.
• Hypotension: Can lower blood pressure excessively, particularly in patients with severe aortic stenosis. Usually mild and well-tolerated given the gradual onset.
• Worsening angina or heart attack at initiation: Rarely, calcium channel blocker initiation can precipitate angina worsening or MI, particularly in patients with severe obstructive coronary artery disease.
• Hepatic impairment: Amlodipine is extensively metabolized by the liver; hepatic impairment can significantly increase exposure. Start at 2.5 mg in these patients.
• Drug interactions: Cyclosporine and tacrolimus levels may be increased by amlodipine. Simvastatin exposure is increased when co-administered with amlodipine; simvastatin dose should be limited to 20 mg daily.
• Pregnancy: Can cause fetal harm. Not recommended during pregnancy, particularly in the second and third trimesters.