Amlodipine is well absorbed following oral administration with peak blood concentrations occurring after 6 to 12 hours. The bioavailability is about 60 to 65%. Amlodipine is reported to be about 97.5% bound to plasma proteins. It has prolonged terminal elimination half-life of 35 to 50 hours and steady-state plasma concentrations are not achieved until 7 to 8 days of administration. Amlodipine is extensively metabolized in the liver; metabolites are mostly excreted in urine together with less than 10% of dose as unchanged drug.
Used in the treatment of mild to moderate hypertension in case of inadequate control with monotherapy.
Hypertension, stable and Prinzmetal's angina Initially, 5 mg once daily. Increase to 10 mg once daily if necessary.
Hypersensitivity. Cardiogenic shock, recent MI, acute unstable angina and chronic stable angina attack. Pregnancy.
Patients with hypotension, poor cardiac reserve, heart failure, volume depletion; severe aortic stenosis; hepatic & renal impairment; renal artery stenosis. Sudden withdrawal may exacerbate angina. Discontinue if ischemic pain following administration occurs. Monitor serum potasisum concentration. Avoid concomitant use with potassium-sparing diuretics. Hepatic and renal impairment. Lactation.
Dizziness, flushing, headache, hypotension, peripheral edema, tachycardia, palpitations. Nausea, GI disturbances, increased micturition frequency, lethargy, eye pain, mental depression. Paradoxical increase in ischemic chest pain at the start of treatment. Rashes, fever, abnormalities in liver function (cholestasis), hyperplasia, myalgia, tremor, impotence.
May enhance antihypertensive effects of other antihypertensives eg, β-blockers, aldesleukin, antipsychotics, quinidine, carbamazepine, phenytoin, rifampicin, cimetidine and erythromycin.
Store at temperatures not exceeding 30°C.
Tab 5 mg x 30's. 10 mg x 30's.