Amlopidine (Norvasc)

A long-acting calcium channel blocker (dihydropyridine (DHP) class) used as an anti-hypertensive and in the treatment of angina.

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.

Acts by relaxing the smooth muscle in the arterial wall, decreasing total peripheral resistance and reducing blood pressure.

Amlopidine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells.

Well absorbed by the oral route with a mean bioavailability of approximately 60%.

Renal elimination is the major route of excretion with about 60% of an administered dose recovered in urine, largely as inactive pyridine metabolites.

Mean half-life of 33 h.

In angina it increases blood flow to the heart muscle.

Amlodipine is used in the management of hypertension, and coronary artery disease.

Adverse side effects include: peripheral edema in 8.3% of users, fatigue in 4.5% of users, dizziness, palpitations, and nausea, gynecomastia, impotence, depression, insomnia, tachycardia, gingival enlargement.

Rarely associated with behavior disorders, hepatitis, and jaundice.

Very rarely associated with hyperglycemia, tremor,and Stevens–Johnson syndrome.

Can increase frequency and severity of angina or actually cause a myocardial infarction, on rare occasions in patients with severe coronary artery disease.

The qbove phenomenon usually occurs when first starting amlodipine, or at the time of dosage increase

May be associated with excessive lowering of blood pressure during initiation of treatment.

Rarely, associated with CHF, usually in patients already on a beta blocker.

Does not affect serum calcium levels.

A peripheral arterial vasodilator that acts directly on vascular smooth muscle to cause a reduction in peripheral vascular resistance and reduction in blood pressure.

With exertional angina, it reduces the total peripheral resistance (afterload) against which the heart works and lowers myocardial oxygen demand.

Blocks constriction and restores blood flow in coronary arteries and arterioles in response to calcium, potassium, epinephrine, serotonin, and thromboxane A2 analog.

Inhibits coronary spasm and is effective in vasospastic angina.

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