Difference between revisions of "Amlodipine"
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Systematic (IUPAC) name | |
---|---|
(RS)-3-ethyl 5-methyl 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate | |
Clinical data | |
Pregnancy category | |
Routes of administration | Oral (tablets) |
Legal status | |
Legal status | |
Pharmacokinetic data | |
Bioavailability | 64 to 90% |
Metabolism | HepaticNikhil and Nilesh filed a patent on amlodipine |
Biological half-life | 30 to 50 hours |
Excretion | Renal |
Identifiers | |
CAS Number | 88150-42-9 |
ATC code | C08CA01 (WHO) |
PubChem | CID 2162 |
DrugBank | APRD00520 |
ChemSpider | 2077 |
Chemical data | |
Formula | C20H25ClN2O5 |
Molar mass | 408.879 g/mol[[Script error: No such module "String".]] |
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Amlodipine (as besylate, mesylate or maleate) is a long-acting calcium channel blocker (dihydropyridine class) used as an anti-hypertensive and in the treatment of angina. Like other calcium channel blockers, amlodipine acts by relaxing the smooth muscle in the arterial wall, decreasing total peripheral resistance and hence reducing blood pressure; in angina it increases blood flow to the heart muscle.
Contents
Indications
Cautions
Contraindications
Amlodipine causes vasodilatation, which in patients with severe aortic stenosis, can result in reduced cardiac output.
There is not absolute consensus about the contraindication, because if the patient has hypertension, his stenosis cannot be very severe, otherwise he would not have sufficient output to allow hypertension.[1]
Side effects
Some side effects of the use of amlodipine may be:[2]
- 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, gingival enlargement - 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
Dose
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- Hypertension or angina: 2.5 to 10 mg once daily (initial treatment can start as low as 2.5 mg per day, titrate up to 10 mg/day as necessary).
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.
The efficacy and tolerability of a fixed-dose combination of amlodipine 5 mg and perindopril 4 mg, an angiotensin converting enzyme (ACE) inhibitor, have recently been confirmed in a prospective, observational multicentre trial of 1250 hypertensive patients.[3]
Drug metabolism and excretion
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Amlodipine is almost entirely metabolised to inactive metabolites. 10% of the parent substance and 60% of the metabolites are excreted in urine.
Stereoisomerism
Amlodipine is a chiral calcium antagonist, currently on the market and in therapeutic use as a racemate [1:1 mixture of (R)-(+)- and (S)-(–)-amlodipine][4]. A method for the semi-preparative chromatographic purification of the enantiomers (S)-(–)-amlodipine and (R)-(+)-amlodipine has been reported.[5]
Patent loss
Pfizer patent protection on Norvasc lasted until 2007. Total patent expiration occurred later in 2007.[6] A number of generic versions are available.
Brand names
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Amlodipine is marketed as:
- Norvasc by Pfizer in North America, some European countries, China, and Japan
- Norvasc and Perivasc in Australia
- Istin in the United Kingdom and Ireland
- Agen by Zentiva in the Czech Republic
- Amdipin in Colombia by Laboratorios Lafrancol
- Amlodine by Dainippon Sumitomo Pharmaceuticals in Japan, and in Philippines by Westfield Pharmaceuticals, a division of InnoGen
- Amdepin by Cadila Pharmaceuticals in India
- Dailyvasc by Xeno Pharmaceuticals
- Aken in Mexico by Kendrick Farmaceutica
- Lopin in Bangladesh by Edruc Ltd
- Amlopine in Thailand by Berlin (Thailand) Pharmaceutical Industry Co Ltd
- Amcard in Bangladesh by Apex Pharma Ltd
- Hipril is a combination of lisinopril with amlodipine (5 mg each) in India by velavan
See also
References
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External links
- Norvasc
- Istin - Summary of Product Characteristics from the electronic Medicines Compendium
- U.S. National Library of Medicine: Drug Information Portal - Amlodipine
bg:Амлодипин de:Amlodipin es:Amlodipina fa:آملودیپین fr:Amlodipine it:Amlodipina hu:Amlodipin nl:Amlodipine ja:アムロジピン pl:Amlodypina pt:Anlodipino ru:Амлодипин
uk:Амлодипін- ↑ Does it matter how severe is the stenosis? NHS July 19, 2006
- ↑ Source: Sandoz product information sheet
- ↑ Bahl VK, Jadhav UM, Thacker HP (2009). "Management of hypertension with the fixed combination of perindopril and amlodipine in daily clinical practice: results from the STRONG prospective, observational, multicenter study". Am J Cardiovasc Drugs. 9 (3): 135–42. doi:10.2165/00129784-200909030-00001. PMID 19463019.
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- ↑ Kennedy, Val Brickates (2007-03-22). "Pfizer loses court ruling on Norvasc patent". MarketWatch.
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