CVnor

Amlodipine

Amlodipine

Composition:

CVnor-5: Each tablet contains Amlodipine Besilate BP equivalent to Amlodipine 5 mg.

CVnor-10: Each tablet contains Amlodipine Besilate BP equivalent to Amlodipine 10 mg.

 

Description:

Amlodipine selectively inhibits the transmembrane influx of calcium ions into the vascular smooth and cardiac muscle. A decrease in intracellular Calcium inhibits the contractile of the myocardial smooth muscle cells. This results in the dilation of the coronary and systemic arteries with a greater pharmacological effect on the vascular smooth muscle than the cardiac muscle. The ultimate effect of Amlodipine is a reduction in peripheral vascular resistance and reduction in blood pressure.

In patient with angina, the exact mechanism of action has not been fully explained. In patients that experience exertion angina, Amlodipine decreases the total peripheral resistance or after load which decreases the myocardial oxygen demand when a person is exercising. Amlodipine inhibits coronary spasms of Prinzmetal’s or variant angina by blocking and restore blood flow in coronary arteries and arterioles.

Indications:

Hypertension, prophylaxis of angina.

Dosage and Administration:

Hypertension or angina, initially 5 mg once daily; max. 10 mg once daily.

Warning:

Increased Angina and/or Myocardial Infarction: Rarely, patients, particularly those with severe obstructive coronary artery disease, have developed documented increased frequency, duration and/or severity of angina or acute myocardial infarction on starting calcium channel blocker therapy or at the time of dosage increase. The mechanism of this effect has not been elucidated.

Precautions:

General: Since the vasodilation induced by Amlodipine is gradual in onset, acute hypotension has rarely been reported after oral administration. Nonetheless, caution as with any other peripheral vasodilator, should be exercised when administering Amlodipine, particularly in patients with severe aortic stenosis.

 

Use in Patients with Congestive Heart Failure: In general, calcium channel blockers should be used with caution in patients with heart failure.

Beta-Blocker Withdrawal: Amlodipine is not a beta-blocker and therefore gives no protection against the dangers of abrupt beta-blocker withdrawal; any such withdrawal should be gradualy reduction of the dose of beta-blocker.

Patients with Hepatic Failure: Since Amlodipine is extensively metabolized by the liver and the plasma elimination half-life (t ½) is 56 hours in patients with impaired hepatic function, caution should be exercised when administering Amlodipine to patients with severe hepatic impairment.

Carcinogenesis, Mutagenesis, Impairment of Fertility:

There was no effect on the carcinogenesis, mutagenesis of impairment of fertility of rats treated orally with Amlodipine Besilate.

Paediatric Use: The effect of Amlodipine on blood pressure in patients less than 6 years of age is not known.

Geriatric Use: Clinical studies of Amlodipine did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.  In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy. Elderly patients have decreased clearance of amlodipine with a resulting increase of AUC of approximately 40-60% and a lower initial dose may be required.

 

Contraindications:

Amlodipine is contraindicated in patients with known sensitivity to Amlodipine.

 

 Side Effects:

The most commonly reported side effects of Amlodipine are headache,edema, rash, fatigue, nausea, flushing and dizziness.

Use in Pregnancy and Lactation :

Amlodipine is pregnancy category C. Animal reproduction studies have been shown to an adverse effect on the fetus even there has not been any adequate and well-controlled studies in pregnant women. Amlodipine may be used during pregnancy is the potential benefits justify the potential risks to the fetus. There is no known information if amlodipine is excreted in human milk. It is recommended that breast-feeding be discontinued during administration of Amlodipine.

Overdosage:

There is no well documented experience with amlodipine overdosage. Gastric lavage may be worthwhile. Available data suggest that gross overdosage could result in excessive peripheral vasodilation with subsequent marked and probably prolonged systemic hypotension. Clinically significant hypotension due to amlodipine overdosage calls for active cardiovascular support. Intravenous calcium gluconate may be beneficial in reversing the effects of calcium channel blockade. Since amlodipine is highly protein-bound, dialysis is not likely to be of benefit.

Storage:

Store in a cool & dry place, protect from light and moisture. Keep out of the reach of children.

Pack Size:

CVnor-5: Each box contains 3 X 10’s tablet in blister pack.

CVnor-10: Each box contains 3 X 10’s tablet in blister pack