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Amlodipine



Amlodipine
Systematic (IUPAC) name
3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(2-
chlorophenyl)-1,4-dihydro-6-methyl-3,5- pyridinedicarboxylate
Identifiers
CAS number 88150-42-9
ATC code C08CA01
PubChem 2162
DrugBank APRD00520
Chemical data
Formula C20H25ClN2O5 
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 (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.

Additional recommended knowledge

Contents

Indications

Cautions

Contra-indications

Side effects

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

Dose

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. [2]

References

  1. ^ Source: Sandoz product information sheet
  2. ^ okpatents.com/.../patent_loss_res
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Amlodipine". A list of authors is available in Wikipedia.
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