Amlodipine

What it is and how it works

Mechanism of Action Amlodipine is a dihydropyridine calcium antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Experimental data suggest that 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 extracellular calcium ions into these cells through specific ion channels. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells.

Indications

Amlodipine besylate tablets, USP is a calcium channel blocker and may be used alone or in combination with other antihypertensive and antianginal agents for the treatment of: Hypertension Amlodipine besylate tablets, USP are indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. Coronary Artery Disease Chronic Stable Angina Vasospastic Angina (Prinzmetal’s or Variant Angina) Angiographically Documented Coronary Artery Disease in patients without heart failure or an ejection fraction < 40% Hypertension Amlodipine besylate tablets, USP are indicated for the treatment of hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions. These benefits have been seen in controlled trials of antihypertensive drugs from a wide variety of pharmacologic classes including amlodipine besylate tablets.

Dosage and administration (summary)

Adult recommended starting dose: 5 mg once daily with maximum dose 10 mg once daily. Small, fragile, or elderly patients, or patients with hepatic insufficiency may be started on 2.5 mg once daily. Pediatric starting dose: 2.5 mg to 5 mg once daily. Important Limitation: Doses in excess of 5 mg daily have not been studied in pediatric patients. Adults The usual initial antihypertensive oral dose of amlodipine besylate tablets is 5 mg once daily, and the maximum dose is 10 mg once daily.

Contraindications

Amlodipine besylate tablets are contraindicated in patients with known sensitivity to amlodipine. Known sensitivity to amlodipine

Warnings and precautions

Symptomatic hypotension is possible, particularly in patients with severe aortic stenosis. However, acute hypotension is unlikely. Worsening angina and acute myocardial infarction can develop after starting or increasing the dose of amlodipine besylate tablets, particularly in patients with severe obstructive coronary artery disease. Titrate slowly in patients with severe hepatic impairment. Hypotension Symptomatic hypotension is possible, particularly in patients with severe aortic stenosis. Because of the gradual onset of action, acute hypotension is unlikely.

Pregnancy

Pregnancy Risk Summary The limited available data based on post-marketing reports with amlodipine use in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage. There are risks to the mother and fetus associated with poorly controlled hypertension in pregnancy .

Storage and supply

2.5 mg Tablets Amlodipine besylate-2.5 mg Tablets (amlodipine besylate, USP equivalent to 2.5 mg of amlodipine per tablet) are supplied as white, round, biconvex, beveled edged tablets debossed with T on one side and 143 on the other and supplied as follows: NDC 76282-507-90 Bottle of 90 NDC 76282-507-05 Bottle of 500 NDC 76282-507-10 Bottle of 100…

Source: Amlodipine Besylate (Amlodipine Besylate) — US FDA prescribing information, 2022-03-12, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.