Amlodipine detailed information
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| Amlodipine detailed information
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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 | |
| Identifiers | |
| CAS number | |
| ATC code | C08 |
| PubChem | |
| DrugBank | |
| 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. | |
| Legal status | |
| Routes | Oral (tablets) |
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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
Contra-indications
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
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. [2]
References
- ↑ Source: Sandoz product information sheet
- ↑ okpatents.com/.../patent_loss_res
External links
- Istin - Summary of Product Characteristics from the electronic Medicines Compendium.
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
