Amlodipine detailed information: Difference between revisions

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{{drugbox |
#REDIRECT [[Amlodipine#Pharmacology]]
|IUPAC_name = 3-[[ethyl]]-5-[[methyl]]-2-(2-[[amino]]ethoxymethyl)-4-(2-<br>chloro[[phenyl]])-1,4-dihydro-6-methyl-3,5- [[pyridine]]di[[carboxylate]]
|image=Amlodipine svg.png
|CAS_number = 88150-42-9
| ATC_prefix=C08
| ATC_suffix=CA01
| PubChem=2162
| DrugBank=APRD00520
| C=20 | H=25 | Cl=1 | N=2 | O=5
|molecular_weight = 408.879 g/mol
|bioavailability = 64 to 90%
|metabolism = [[Liver|Hepatic]]
|elimination_half-life = 30 to 50 hours
|excretion = [[Kidney|Renal]]
|pregnancy_AU = C
|pregnancy_US = C
|legal_UK = POM
|legal_US = Rx-only
|routes_of_administration = Oral (tablets)
}}
{{CMG}}
 
 
 
==[[Amlodipine (patient information)|For patient information, click here]]==
 
'''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 pectoris|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 pectoris|angina]]
 
==Cautions==
*[[hepatic]] impairment
*[[pregnancy]]
 
==Contra-indications==
*[[cardiogenic shock]]
*[[unstable angina]]
*significant [[aortic stenosis]]
*[[breast feeding]]
 
==Side effects==
Some side effects<ref>Source: [[Sandoz]] product information sheet</ref> of the use of amlodipine may be:
* Very often: [[peripheral edema]] ([[foot|feet]] and [[ankle]]s) - in 1 of 10 users
* Often: [[dizziness]], [[palpitations]], [[muscle]], [[stomach]] or [[headache]], [[dyspepsia]], [[nausea]] - in 1 in 100 users
* Sometimes: [[blood]] disorders, development of [[breast]]s in [[man|men]] ([[gynecomastia]]), [[impotence]], [[Clinical depression|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 pectoris|angina]]: 5 or 10 [[milligram|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.  <ref>[http://www.okpatents.com/phosita/archives/2005/02/patent_loss_res.html okpatents.com/.../patent_loss_res]</ref>
 
==References==
{{reflist|2}}
 
==External links==
*[http://emc.medicines.org.uk/emc/assets/c/html/displaydoc.asp?documentid=1466 Istin - Summary of Product Characteristics] from the electronic Medicines Compendium.
 
{{Calcium channel blockers}}
 
[[Category:Calcium channel blockers]]
[[Category:Drugs]]
 
[[de:Amlodipin]]
[[fr:Amlodipine]]
[[hu:Amlodipin]]
[[pt:Amlodipina]]
 
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Latest revision as of 00:06, 22 July 2014