Amlodipine Besilate

FORMULATION:
Each tablet contains:
Amlodipine Besilate        …………..……….     5mg / 10mg
Excipients                       …………..……….     Q.S.

PHARMACOKINETICS;
Amlodipine is well absorbed after oral doses with peak concentrations occurring
after 6 to 12 hours. The bioavailability varies but is usually about 60 to 65%. Amlodipine is reported to be 97.5% bound plasma proteins. It has a prolonged terminal elimination hall-lite of 35 to 50 hours and steady-state plasma concentrations are not achieved until after 7 to 8 days of use.  Amlodipine is extensively metabolized in the liver; metabolites are mostly excreted in urine together with less than 10% of a dose as unchanged drug. Amlodipine is not removed by dialysis.

PHARMACOLOGY:
Amlodipine is a dihydropyridine calcium antagonist that inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle. Amlodipine inhibits calcium 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. 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.

INDICATION:
Use in the management of hypertension and angina pectoris.

DOSAGEAND ADMINISTRATION:
Adult; The usual Initial antihypertensive oral dose of amlodipine is 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 daily and this dose may be used when adding amlodipine to other antihypertensive therapy.

DRUG INTERACTIONS:
Beta-blockers: May cause increased adverse cardiac effects as a result of myocardial depression.
Fentanyl: Severe hypotension or increased fluid volume requirements have occurred with similar drug.

WARNING:
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

PRECAUTION:
Use with caution in patients receiving other peripheral dilators and in those with aortic stenosis, heart failure, or severe hepatic disease.

ADVERSE EFFECTS:
Nausea, headache, flushing, hypotension, abdominal pain, peripheral oedema. fatigue, dizziness, palpitation, rash.

CAUTION:
Foods, Drugs, Devices, and Cosmetics Act prohibits dispensing without prescription.

“For suspected adverse drug reaction, report to the FDA: www.fda.gov.ph.

STORAGE CONDITION:
Store at temperatures not exceeding 300C.
Protect from light.

KEEP ALL MEDICINES OUT OF REACH OF CHILDREN.

AVAILABILITY:
Alul/Alu Blister Pack x (Box of IOO’s).