AMLOKIN

Each film coated tablets contains:

(Amlodipine Besylate IP equivalent to Amlodipine 2.5 mg / 5mg / 10mg / L

Tablet for Oral Use

Amlodipine is a Dihydropyridine Calcium Antagonist (calcium ion antagonist or slow-channel blocker) that inhibits the influx of calcium ions into both vascular smooth muscle and cardiac muscle. The contraction of cardiac muscle and vascular smooth muscle are dependent on the movement of extracellular calcium ions into these cells by specific ion channels. Amlodipine blocks calcium ion influx across cell membranes with selectivity. A stronger effect of amlodipine is exerted on vascular smooth muscle cells than on cardiac muscle cells. Direct actions of amlodipine on vascular smooth muscle result in reduced blood pressure.

Amlodipine has a dilating effect on peripheral arterioles, reducing the total peripheral resistance (afterload) against which the cardiac muscle functions. Since the heart rate remains stable during amlodipine administration, the reduced work of the heart reduces both myocardial energy use and oxygen requirements. Dilatation of the main coronary arteries and coronary arterioles, both in healthy and ischemic areas, is another possible mechanism of amlodipine reduction of blood pressure. The dilatation causes an increase in myocardial oxygen delivery in patients experiencing coronary artery spasm.

Absorption: Amlodipine is absorbed slowly and almost completely from the gastrointestinal tract. Peak plasma concentrations are achieved 6-12 hours after oral administration. The estimated bioavailability of amlodipine is 64-90%. Amlodipine has a half-life of 35-40 h. Steady-state plasma amlodipine levels are achieved after 7-8 days of consecutive daily dosing. Absorption is not affected by food.

Protein Binding: 98%

Distribution: is large and about 21 l/kg

Metabolism: Amlodipine is heavily (approximately 90%) converted to inactive metabolites via hepatic breakdown with 10% of the parent compound and 60% of the metabolites found excreted in the urine. 

• Hypertension
• Coronary artery disease
• Angina
• Myocardial Infraction

ADVERSE REACTION:

Swelling of the hands, feet, ankles, or lower legs, headache, upset stomach, nausea, stomach pain, dizziness or lightheadedness, drowsiness, excessive tiredness, flush, reflex hypotension, gingival hyperplasia, decreases G.I motility leading to constipation

DOSAGE AND ADMINISTRATION:

Hypertension: 5 mg/day PO initially; may be increased by 2.5 mg/day every 7-14 days; not to exceed 10 mg/day

Maintenance: 5-10 mg/day

Angina & Coronary Artery Disease: 5-10 mg/day PO initially

Maintenance: 10 mg/day PO

CONTRAINDICATIONS:

• Hypersensitivity to Amlodipine, Pregnancy and Breast feeding, Cardiogenic shock, Unstable Angina

WARNINGS AND PRECAUTIONS:

• Lower initial dose may be required for patients with hepatic impairment. Consider starting with 2.5 mg/day PO
• Tell your doctor if you have or have ever had heart failure or heart or liver disease
• Tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding

Drug Interaction:

• Additive hypotensive effect may be seen when used concurrently with Fentanyl, other hypertensive, Alcohol, nitrates.
• May increase risk of neurotoxicity when given with lithium