Amlodipine
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Amlodipine
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| Systematic (IUPAC) name | |
| 3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(2- chlorophenyl)-1,4-dihydro-6-methyl-3,5- pyridinedicarboxylate |
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| Identifiers | |
| CAS number | |
| ATC code | C08 |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C20H25ClN2O5 |
| Mol. mass | 408.879 g/mol |
| SMILES | & |
| Pharmacokinetic data | |
| Bioavailability | 64 to 90% |
| Metabolism | Hepatic |
| Half life | 30 to 50 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status | |
| 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.
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[edit] Indications
- hypertension
- prophylaxis of angina
[edit] Cautions
[edit] Contra-indications
[edit] 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
[edit] Dose
- Hypertension or angina: 5 or 10 mg once daily (inital treatment can start as low a 2.5 mg per day).
[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 lasted until 2007. A number of generic versions are now available. Total patent expiration occurred later in 2007.[2]
[edit] References
- ^ Source: Sandoz product information sheet
- ^ Pfizer loses court ruling on Norvasc patent
[edit] External links
- Norvasc
- Istin - Summary of Product Characteristics from the electronic Medicines Compendium
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