Drugs & Medication

Amlodipine
Systematic (IUPAC) name
3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(2- chlorophenyl)-1,4-dihydro-6-methyl-3,5- pyridinedicarboxylate benzenesulfonate
Identifiers
CAS number	88150-42-9
ATC code	C08CA01
PubChem	2162
DrugBank	APRD00520
Chemical data
Formula	C20H25ClN2O5.C6H6O3S
Mol. weight	408.879 g/mol
Pharmacokinetic data
Bioavailability	64 to 90%
Metabolism	Hepatic
Half life	30 to 50 hours
Excretion	Renal
Therapeutic considerations
Pregnancy cat.	C(AU) C(US)
Legal status	POM(UK) ℞-only(US)
Routes	Oral (tablets)

Amlodipine (as besylate, mesylate or maleate) is a long-acting calcium channel blocker used as an anti-hypertensive and in the treatment of angina. Amlodipine is marketed as Norvasc® in North America and as Istin® in the United Kingdom as well as under various other names. As other calcium channel blockers, amlodipine acts by relaxing the smooth muscle in the arterial wall, decreasing peripheral resistance and hence improving blood pressure; in angina it improves blood flow to the myocardium. It was developed under the direction of Dr. Simon Campbell.

Contents 1 Indications 2 Cautions 3 Contra-indications 4 Side effects 5 Dose 6 Salts 7 Patent Loss 8 External links

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 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

Source: Sandoz product information sheet

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.

Patent Loss

Pfizer patent protection on Norvasc until 2007. [1]

External links

• Norvasc - Prescription Drug Info Amlodipine Profile
• Istin - Summary of Product Characteristics from the electronic Medicines Compendium