AMLOFIL Tablet

1. Essential hypertension

2. Angina pectoris

3. Vasospastic angina

Dosage

Adults: The usual initial antihypertensive oral dose is 5mg once daily with a maximum dose of 10mg once daily. Small, fragile, or elderly individuals, or patients with hepatic insufficiency may be started on 2.5mg once daily and this dose may be used when adding AMLODIPINE to other antihypertensive therapy. The recommended dose for chronic stable or vasospastic angina is 5/10mg, with the lower dose suggested in the elderly and in patients with hepatic insufficiency. Most patients will require 10mg for adequate effect. The recommended dose range for patients with coronary artery disease is 5-10mg once daily. In clinical studies, the majority of patients required 10mg.

Children: Age 6-17 years is 2.5-5mg once daily. Doses in excess of 5mg daily have not been studied in pediatric patients.

1. Hypersensitivity to dihydropyridine derivatives

2. Pregnancy

3. Care should be taken in patients with sinus node disease, ad in those with aortic stenosis.

Headache, flushing, hypotension, nausea, abdominal pain, peripheral oedema, fatigue, dizziness, palpitation, rash.

ACE inhibitors, Thiazide diuretics: Potentiates effect of these drugs.

Beta Blockers: Best avoided, especially by those with impaired LV function due to depressant effect on myocardial contractibility or AV conduction.

Fentanyl: Severe hypotension or increased fluid volume requirements.

Preganancy

Contraindicated.

Nursing Mothers

It is not known whether amlodipine is excreted in human milk. In the absence of this information, it is recommended that nursing be discontinued while AMLODIPINE is administered.

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 AMODIPINE, particularly in patients with severe aortic stenosis.

Increased angina and/or myocardial infarction: Rarely, patients, particularly those with severe obstructive coronary artery disease, have developed 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 been elucidated.

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 moth 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 vitro but 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 receptor binding site, resulting in a gradual onset of effect. Amlodipine is a peripheral 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.