Amlodipine Besylate

Amlodipine Besylate

Class:Calcium Antagonist

Mechanism of action

Inhibits calcium ion from entering the “slow channels” or select voltage-sensitive areas of vascular smooth muscle and myocardium during depolarization,producing a relaxation of coronary vascular smooth muscle and coronary vasodilation;increases myocardial oxygen delivery in patients with vasospastic angina.

Pharmacokinetics

Onset of action:30-50 minutes.Peak effect:6-12 hours.Duration:24 hours.Absorption:oral:well absorbed.Protein binding:93 percent.Metabolism:hepatic.Half life:30-50 hours.Elimination:renally.

Indications

Amlodipine is indicated for the first line treatment of hypertension and can be used as the sole agent to control blood pressure in the majority of patients.Patients not adequately controlled on a single antihypertensive agent may benefit from the addition of amlodipine,which has been used in combination with a thiazide diuretics,beta adrenoceptor blocking agent,or an angiotension converting enzyme inhibitor.Amlodipine is indicated for the first line treatment of myocardial ischemia,whether due to fixed obstruction(stable angina) and/or vasospasm/vasoconstriction(prinzmetal’s or variant angina) of coronary vasculature.

Contraindications

Amlodipine is contraindicated in patients with a known sensitivity to dihydropyridine.

Side effects

Headache,edema,fatigue,nausea,flushing and dizziness.

Pregnancy and lactation

Pregnancy risk factor C.No well controlled studies have been conducted in pregnant women.

Drug interaction

Amlodipine has been safely administered with thiazide diuretics,beta-blockers,ACE inhibitors,long acting nitrates,sublingual nitroglycerine,non steroidal anti-inflammatory drugs,antibiotics and oral hypoglycaemic drugs.

Dosage

For both hypertension and angina the usual initial dose is 5mg amlodipine once daily which may be increased to a maximum dose of 10mg depending on the individual patient’s response.

Brands

Tabs.Norvasc 5,10mg,Tabs.Sofvasc,Tabs,Zodip,Tabs.Amodip.