Amlodipine detailed information

Amlodipine detailed information

Clinical data
Pregnancy category	AU: C US: C (Risk not ruled out)
Routes of administration	Oral (tablets)
ATC code	C08CA01 (WHO)
Legal status
Legal status	UK: POM (Prescription only) US: ℞-only
Pharmacokinetic data
Bioavailability	64 to 90%
Metabolism	Hepatic
Elimination half-life	30 to 50 hours
Excretion	Renal
Identifiers
IUPAC name 3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(2- chlorophenyl)-1,4-dihydro-6-methyl-3,5- pyridinedicarboxylate
CAS Number	88150-42-9
PubChem CID	2162
DrugBank	APRD00520
E number	{{#property:P628}}
ECHA InfoCard	{{#property:P2566}}
Chemical and physical data
Formula	C20H25ClN2O5
Molar mass	408.879 g/mol

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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 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

Some trade brands:

Stamlo, Amlodac, Amlong

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 lasts until 2007. A number of generic versions are now available. Total patent expiration will occur later in 2007.

External links

• Istin - Summary of Product Characteristics from the electronic Medicines Compendium.

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