Description

How Supplied

Amlodipine Tablets are presented as forms containing 5 mg Amlodipine (as besylate), 10 Tablets per blister pack, and 3 blisters with a leaflet in a box.

Category

Antianginal;antihypertensive

Mechanism of Action

Amlodipine is a dihydropyridine calcium channel blocking agent. Its selectively inhibits calcium influx across cell membranes in cardiac and vascular smooth muscle, with a greater effect on vascular smooth muscle. Amlodipine is a peripheral arteriolar vasodilator, thus it reduces afterload.

Pharmacokinetics

• Absorption :Slowly and almost completely absorbed from the gastrointestinal tract, absorption not affected by food. Bioavailability is approximately 60 to 65%.
• Half – life: Elimination – mean 35 hours in healthy volunteers, may be prolonged to a mean of 48 hours in hypertensive patients, 65 hours in the elderly, and 60 hours in patients with hepatic function impairment. Not affected by renal function impairment
• Elimination: Renal -59 to 62% (about 5% as unchanged Amlodipine)-

Biliary / fecal : 20 to 25% ; In dialysis – Amlodipine is not removed by hemodialysis.

• Protein binding:very high 95-98%

Pregnancy and Breast – Feeding

FDA pregnancy category C.and it is not known whether amlodipine is distributed into breast milk.

Precautions

• Making regular visit to physician to check progress during therapy.
• Checking with physician before discontinuing medication, gradual dosage reduction may be necessary.
• Discussing exercise or physical exertion limits with physician, reduced occurrence of chest pain may tempt patient to be overactive.
• Checking with physician, if headache occure, continuing or sever.
• Maintaining good dental hygiene and seeing dentist frequently for teeth cleaning to prevent tenderness, bleeding and gum enlargement.
• For use as antihypertensive : Not taking other medications, especially nonprescription sympathomimetics, unless discussed with physician.

Drug interaction

Inform your doctor if you are taking any of the following medicines :Anesthetics, hydrocarbon inhalation; nonsteroidal Anti- inflammatory drugs (NSAID_S), especially indomethacin; Beta – adrenergic blocking agent; Estrogens; Highly protein – bound medications like Anticonvulsant, hydantion; Anticoagulants, coumarin and indandione derivative; Quinine; salicylates; sulfinpyrazone; hypotension- producing medications; lithium; sympathomimetics.

Dosage and adminstration

Usual adult dose :

• Angina,chronic stable or vasospastic or hypertension:5 to 10 mg once a day.

Note : An initial antihypertensive dose of 2.5 mg is recommended for small, fragile, or elderly patients, patients with hepatic function impairment, or when adding amlodipine to other antihypertensive therapy. An initial antianginal dose of 5 mg is recommended for the elderly and for patients with hepatic function impairment.

Usual Pediatric Dose

• Antihypertensive :

Children younger than 6 years of age : safety and efficacy have not been established.

Children 6 years of age and older : oral, 2.5 to 5 mg once daily.

Side Effects

Those indicating need for medical attention

peripheral edema;Dizziness; palpitation;Angina; bradycardia; hypotension; jaundice; orthostatic hypotension.

Those indicating need for medical attention only if they continue or are bothersome

Abdominal pain; flushing; headache; somnolence.Fatigue; nausea.

Storage

Store below 30^˚c , protect from light and moisture . Keep out of reach of children.

Date o revision

September 2013

Manufactured by Pursina pharmaceutical Co. Tehran – Iran