2011/03/16

Amlodipine Besylate For Hypertension

Pharmacology of Amlodipine Besylate :
1. Pharmacodynamics of Amlodipine Besylate
Amlodipine Besylate, a basic Dihydropyridine derivative, inhibits the calcium influx through "slow" channels in peripheral vascular and coronary smooth muscle cells. thus producing marked vasodilatation in peripheral and coronary vascular beds. The mechanism is due to a direct relaxant effect on vascular smooth muscle. Short to medium term clinical trials indicate that Amlodipine is effective both as an antianginal agent in patients with stable angina pectroris and an antihypertensive agent in patients with mild to moderate hypertension.

2. Pharmacokinetics of Amlodipine Besylate
Absorption Amlodipine Besylate
After oral administration of therapeutic doses, Amlodipine Besylate is slowly and almost completelyabsorbed with peak plasma concentration are attained within 6-12 hours post 80%. Absorption of Amlodipine Besylate is unaffected by consumption of food. Steady state plasma levels are reached after 7 -8 dyas of consecutive dosing.
Distribution Amlodipine Besylate
Amlodipine Besylate is > 95% bound to plasma proteins. The volume of distribution is approximately 21L/kg.
Metabolism
Amlodipine Besylate is extensively metabolized by the liver to inactive metabolities.
Excretion Amlodipine Besylate
The terminal plasma elimination half-life is about 35-50 hours and is consistent with once daily dosing. Less than 10% of an oral dose is excreted unchanged. 60% of metabolities are exreted in the urine.

Indication of Amlodipine Besylate
- Treatment of Hypertension
can be used as the sole agent to control blood pressure in the majority of patients. Patients who are not adequately controlled on a single antihypertensive agent may benefit from additional of amlodipine which has been used combination with a Thiazide Diuretic or and angiotensin converting enzyme inhibitor.
-Treatment of Myocardial Ischemia
Whether due fixed obtruction ( Stable angina ) and vasospasm / Vasocontriction of coronary vasculature, Amlodipine Besylate may be used alone as monotherapy or in combination with other antianginal drugs in patients with angina that is refactory nitrates and or adequate doses of B-blocker.

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