Amlive

COMPOSITION

AMLIVE TAB

Each tablet contains:

Amlodipine besilate eqv. To

 Amlodipine                            2.5mg/5mg/10mg   

               

DESCRIPTION

AMLIVE contains amlodipine belonging to Calcium Channel Blockers, an important group of drugs for treatment of hypertension. Amlodipine inhibits calcium ion influx across cell membranes selectively, with a greater effect on vascular smooth muscle cells than on cardiac muscle cells.

PHARMACOLOGY

Pharmacodynamics

Hemodynamics: Following administration of therapeutic doses to patients with hypertension, amlodipine produces vasodilation resulting in a reduction of supine and standing blood pressures. These decreases in blood pressure are not accompanied by a significant change in heart rate or plasma catecholamine levels with chronic dosing.

Pharmacokinetics

After oral administration of therapeutic doses of amlodipine, absorption produces peak plasma concentrations between 6 and 12 hours. Absolute bioavailability has been estimated to be between 64 and 90%. The bioavailability of amlodipine is not altered by the presence of food. Amlodipine is extensively (about 90%) converted to inactive metabolites via hepatic metabolism with 10% of the parent compound and 60% of the metabolites excreted in the urine. Ex vivo studies have shown that approximately 93% of the circulating drug is bound to plasma proteins in hypertensive patients. Elimination from the plasma is biphasic with a terminal elimination half-life of about 30-50 hours. Steady-state plasma levels of amlodipine are reached after 7 to 8 days of consecutive daily dosing.

Indications
AMLIVE is indicated for hypertension, chronic stable angina and vasospastic angina (Prinzmetal's or variant angina). AMLIVE may be used as monotherapy or in combination with other antihypertensive or antianginal drugs.

DOSAGE AND ADMINISTRATION

Hypertension

Initial dose of 5 mg once daily, with a maximum dose of 10 mg once daily. Small, fragile or elderly individuals or patients with hepatic insufficiency may be started on 2.5 mg once daily and this dose may be used when adding amlodipine to other anti-hypertensive therapy.

Chronic stable or vasospastic angina

5-10 mg with a lower dose (2.5 mg) in the elderly and in patients with hepatic insufficiency.

Co-administration with other antihypertensives and/or antianginal drugs

Amlodipine has been safely administered with thiazides, ACE inhibitors, beta-blockers, long acting nitrates and/or sublingual nitroglycerin.

Children

The effective antihypertensive oral dose in paediatric patients (6-17 years) is 2.5 mg to 5 mg once daily. Doses in excess of 5 mg daily have not been studied in paediatric patients.

CONTRAINDICATIONS

Amlodipine is contraindicated in patients with known hypersensitivity to amlodipine.

WARNING AND PRECAUTION

AMLIVE should be use cautiously in patients with congestive heart failure, hepatic impairment, pregnant, lactation and in children.

ADVERSE EFFECTS

Amlodipine is well tolerated. Side effects include headache, oedema, fatigue, somnolence, nausea, abdominal pain, flushing, palpitations and dizziness.

Less commonly observed are pruritus, rash, dyspnoea, asthenia, muscle cramps and dyspepsia. Rarely, myocardial infarction and chest pain have been reported.

DRUG INTERACTIONS

In clinical trials, amlodipine has been safely administered with thiazide diuretics, beta-blockers, angiotensin converting enzyme inhibitors, long acting nitrates, sublingual nitroglycerin, digoxin, warfarin, non-steroidal anti-inflammatory drugs, antibiotics and oral hypoglycemic drugs.