AMLODIPINE BESYLATE USP Tablet

- Treatment of angina pectoris,

- Treatment of mild to moderate hypertension, alone or in combination with other antihypertensives.

Dosage and Administration

Route of administration: Oral.

Hypertension and angina Pectoris:

Adults: An initial dose of 5mg once daily is recommended which may be increased to 10mg once a day after 10-14 days of therapy if there is no improvement.

No dose reduction is required when adding Amlodipine to thiazide diuretics, beta-blockers, or angiotensin converting enzyme inhibitors.

In patients with hypersensitivity to dihydropyridine derivatives, amlodipine or any of the excipients.

The most commonly reported adverse reactions are somnolence, dizziness, headache, palpitations, flushing, abdominal pain, nausea, ankle swelling, oedema and fatigue.

Amlodipine has been safely administered with thiazide diuretics, alpha blockers, beta blockers, angiotensin-converting enzyme inhibitors, long-acting nitrates, sublingual glyceryl trinitrate, NSAIDs, antibiotics, and oral hypoglycaemic drugs.

Atorvastatin: Co-administration of multiple 10mg doses of amlodipine with 80mg of atorvastatin resulted in no significant change in the steady state pharmacokinetic parameters of atorvastatin.

Digoxin: Co-administration of amlodipine with digoxin did not change serum digoxin levels of digoxin renal clearance in normal volunteers.

Warfarin: In healthy male volunteers, the co-administration of amlodipine does not significantly alter the effect of warfarin on prothrombin response time. Co-administration of amlodipine with warfarin did not change the warfarin prothrombin response time.

Safety in pregnancy and lactation has not been established.

Use in Elderly:

Amlodipine clearance is decreased (40-60%) in the elderly, which results in increases of amlodipine concentration in the area under the AUC and elimination half-life. Therefore, elderly patients should start Amlodipine therapy at a lower dose.

Use in Renal Failure:

Although Amlodipine is excreted primarily via the kidneys, mild renal impairment does not appear to have an effect on the plasma concentration. Severe renal impairment may however require a dosage reduction. Amlodipine is not dialysable.

Use in impaired Hepatic Function:

The half-life of Amlodipine is significantly prolonged in patients with impaired hepatic function. Amlodipine should therefore be administered at lower doses in these patients.

Use in Children:

Safely and efficacy have not been established.

Use in Heart Failure:

An increased incidence of pulmonary oedema has been reported. Amlodipine may have negative inotropic effect. AUC of Amlodipine may increase in patients with heart failure.

Category: Calcium channel blocker

Amlodipine is a dihydropyridine calcium channel blocker. It inhibits the transmembrane influx of calcium ions into cardiac and vascular smooth muscle without affecting serum calcium concentrations. Direct relaxation of vascular smooth muscle forms the basis of the antihypertensive action.

In angina pectoris, amlodipine acts as a peripheral arteriolar vasodilator resulting in a reduction in total peripheral resistance (afterload). Myocardial energy and oxygen requirements are reduced. Amlodipine exerts its activity by binding to the dihydropyridine binding sites. It exerts minimal action on cardiac conduction, contraction and heart rate.