Norvasc
Amlodipine (as besylate, mesylate or maleate) is a long-acting calcium channel blocker (dihydropyridine) used as an anti-hypertensive and in the treatment of angina. As other calcium channel blockers, amlodipine acts by relaxing the smooth muscle in the arterial wall, decreasing peripheral resistance and hence reducing blood pressure; in angina it increases blood flow to the heart muscle.

Amlodipine is marketed as Norvasc® in North America and as Istin® in the United Kingdom by Pfizer as well as under various other names.

Indications
hypertension
prophylaxis of angina

Cautions
hepatic impairment
pregnancy

Contra-indications
cardiogenic shock
unstable angina
significant aortic stenosis
breast feeding

Side effects
Some side effects[1] of the use of amlodipine may be:

Very often: peripheral edema (feet and ankles) - in 1 of 10 users
Often: dizziness, palpitations, muscle, stomach or headache, dyspepsia, nausea - in 1 in 100 users
Sometimes: blood disorders, development of breasts in men (gynecomastia), impotence, depression, insomnia, tachycardia - in 1 in 1,000 users
Rarely: erratic behavior, hepatitis, jaundice - in 1 in 10,000 users
Very rarely: hyperglycemia, tremor, Stevens-Johnson syndrome - in 1 in 100,000 users

Dose
Hypertension or angina: 5 or 10 mg once daily.

Salts
In the United Kingdom tablets of amlodipine from different suppliers may contain different salts. The strength of the tablets is expressed in terms of amlodipine base. i.e. without the salt. Tablets containing different salts are therefore considered interchangeable.

Drug Metabolism and Excretion
Amlodipine is almost entirely metabolised to inactive metabolites. Ten per cent of the parent substance and 60% of the metabolites are excreted in urine.

Patent loss
Pfizer patent protection on Norvasc lasted until 2007. A number of generic versions are now available. Total patent expiration occurred later in 2007.