Amlodipine Besylate (24 brand names, 5 dosage forms, 1 route)
Available dosage forms: TABLET, CAPSULE, FOR SOLUTION, SOLUTION, TABLET, ORALLY DISINTEGRATING.
Routes of administration: ORAL.
Brand Names
- AMLODIPINE AND OLMESARTAN MEDOXOMIL
- AMLODIPINE BESYLATE
- AMLODIPINE BESYLATE AND ATORVASTATIN CALCIUM
- AMLODIPINE BESYLATE AND BENAZEPRIL HYDROCHLORIDE
- AMLODIPINE BESYLATE AND VALSARTAN
- AMLODIPINE BESYLATE, VALSARTAN AND HYDROCHLOROTHIAZIDE
- AMLODIPINE BESYLATE; BENAZEPRIL HYDROCHLORIDE
- AMTURNIDE
- AZOR
- CADUET
- CONSENSI
- EXFORGE
- EXFORGE HCT
- LOTREL
- NORLIQVA
- NORVASC
- OLMESARTAN MEDOXOMIL, AMLODIPINE AND HYDROCHLOROTHIAZIDE
- PRESTALIA
- SDAMLO
- TEKAMLO …and 4 more
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. Negative inotropic effects can be detected in vitrobut such effects have not been seen in intact animals at therapeutic doses. Serum calcium concentration is not affected by amlodipine. Within the physiologic pH range, amlodipine is an ionized compound (pKa=8.6), and its kinetic interaction with the calcium channel receptor is characterized by a gradual rate of association and dissociation with the receptor binding site, resulting in a gradual onset of effect. Amlodipine is a peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure. The precise mechanisms by which amlodipine relieves angina have not been fully delineated, but are thought to include the following: Exertional Angina: In patients with exertional angina, amlodipine besylate reduces the total peripheral resistance (after load) against which the heart works and reduces the rate pressure product, and thus myocardial oxygen demand, at any given level of exercise. Vasospastic Angina: Amlodipine besylate has been demonstrated to block constriction and restore blood flow in coronary arteries and arterioles in response to calcium, potassium epinephrine, serotonin, and thromboxane A2 analog in experimental animal models and in human coronary vessels in vitro. This inh
Overdosage
Overdosage might be expected to cause excessive peripheral vasodilation with marked hypotension and possibly a reflex tachycardia. In humans, experience with intentional overdosage of amlodipine besylate is limited. Single oral doses of amlodipine maleate equivalent to 40 mg amlodipine/kg and 100 mg amlodipine/kg in mice and rats, respectively, caused deaths. Single oral amlodipine maleate doses equivalent to 4 or more mg amlodipine/kg or higher in dogs (11 or more times the maximum recommended human dose on a mg/m 2basis) caused a marked peripheral vasodilation and hypotension. If massive overdose should occur, initiate active cardiac and respiratory monitoring. Frequent blood pressure measurements are essential. Should hypotension occur, provide cardiovascular support including elevation of the extremities and the judicious administration of fluids. If hypotension remains unresponsive to these conservative measures, consider administration of vasopressors (such as phenylephrine) with attention to circulating volume and urine output. As amlodipine besylate is highly protein bound, hemodialysis is not likely to be of benefit.