Amlodipine

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Amlodipine
Systematic (IUPAC) name
3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(2- chlorophenyl)-1,4-dihydro-6-methyl-3,5- pyridinedi carboxylate benzene sulfonate
Identifiers
CAS number	88150-42-9
ATC code	C08CA01
PubChem	2162
DrugBank	APRD00520
Chemical data
Formula	C₂₀H₂₅Cl N₂O₅
Mol. mass	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. 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 as well as under various other names. It was developed under the direction of Dr. Simon Campbell.

1 Indications
2 Cautions
3 Contra-indications
4 Side effects
5 Dose
6 Salts
7 Drug Metabolism and Excretion
8 Patent loss
9 External links

[edit] Indications

hypertension
prophylaxis of angina

[edit] Cautions

hepatic impairment
pregnancy

[edit] Contra-indications

[edit] 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

[edit] Dose

Hypertension or angina: 5 or 10 mg once daily.

[edit] 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.

[edit] 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.

[edit] Patent loss

Pfizer patent protection on Norvasc until 2007. [1]

[edit] External links

Istin - Summary of Product Characteristics from the electronic Medicines Compendium

v • d • e Calcium channel blockers (C08)
Dihydropyridines	Amlodipine, Felodipine, Isradipine, Lacidipine, Lercanidipine, Nicardipine, Nifedipine, Nimodipine, Nisoldipine
Phenylalkylamines	Verapamil
Benzothiazepines	Diltiazem