Amlodipine, sold under the brand name Norvasc among others, is a calcium channel blocker medication used to treat high blood pressure, coronary artery disease (CAD)[10] and variant angina (also called Prinzmetal angina or coronary artery vasospasm, among other names).
[10] Common side effects include swelling, feeling tired, abdominal pain, and nausea.
[17] Amlodipine is used in the management of hypertension (high blood pressure)[18] and coronary artery disease in people with either stable angina (where chest pain occurs mostly after physical or emotional stress)[19] or vasospastic angina (where it occurs in cycles) and without heart failure.
[21] Amlodipine along with other calcium channel blockers are considered the first choice in the pharmacological management of Raynaud's phenomenon.
Those with impaired liver function are unable to metabolize amlodipine to its full extent, giving it a longer half-life than typical.
[7][30] Peripheral edema (fluid accumulation in the tissues) occurs at rate of 10.8% at a 10-mg dose (versus 0.6% for placebos), and is three times more likely in women than in men.
The increased dilation allows for more blood, which is unable to push through to the relatively constricted postcapillary venules and vessels; the pressure causes much of the plasma to move into the interstitial space.
[31] Amlodipine-association edema can be avoided by adding ACE inhibitors or angiotensin II receptor antagonist.
[10] Of the other dose-dependent side effects, palpitations (4.5% at 10 mg vs. 0.6% in placebos) and flushing (2.6% vs. 0%) occurred more often in women; dizziness (3.4% vs. 1.5%) had no sex bias.
[7] Common but not dose-related adverse effects are fatigue (4.5% vs. 2.8% with a placebo), nausea (2.9% vs. 1.9%), abdominal pain (1.6% vs. 0.3%), and drowsiness (1.4% vs.
[7] Side effects occurring less than 1% of the time include: blood disorders, impotence, depression, peripheral neuropathy, insomnia, tachycardia, gingival enlargement, hepatitis, and jaundice.
However, depending on the situation, amlodipine inhibits constriction and restores blood flow in coronary arteries as a result of its acting directly on vascular smooth muscle, causing a reduction in peripheral vascular resistance and a consequent reduction in blood pressure.
[10] Amlodipine and other dihydropyridine calcium channel blockers are associated with primary open angle glaucoma.
[40] The FDA issued a warning to limit simvastatin to a maximum dose of 20 mg if taken with amlodipine based on evidence from the SEARCH trial.
[43][44] Amlodipine has an inhibitory effect on calcium influx in smooth muscle cells to inhibit contraction.
[7] It is slowly metabolized in the liver by CYP3A4, with its amine group being oxidized and its side ester chain being hydrolyzed, resulting in an inactive pyridine metabolite.
[54] Renal elimination is the major route of excretion with about 60% of an administered dose recovered in urine, largely as inactive pyridine metabolites.
Amlodipine is also used to treat congestive heart failure due to mitral valve regurgitation in dogs.