Atorvastatin
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| [R-(R*, R*)]-2-(4-fluorophenyl)-beta, delta-dihydroxy-5- (1-methylethyl)-3-phenyl-4- [(phenylamino)carbonyl]-1H- pyrrole-1-heptanoic acid IUPAC name | |
| CAS number 134523-00-5 | ATC code C10AA05 |
| Chemical formula | (C33H34FN2O5)2Ca•3H2O |
| Molecular weight | 1209.42 |
| Bioavailability | 12% |
| Metabolism | Liver |
| Elimination half life | 14 hours |
| Excretion | Bile |
| Pregnancy category | X (USA) D (Aust) |
| Legal status | Schedule 4 (Aust) |
| Routes of administration | oral |
In medicine and pharmacology, atorvastatin (Lipitor® or atorvastatin calcium) is a member of the drug class of statins, used for lowering cholesterol and thereby preventing cardiovascular disease. Atorvastatin inhibits a rate-determining enzyme located in hepatic tissue used in cholesterol synthesis, which lowers the amount of cholesterol produced. This also has the effect of lowering the total amount of LDL cholesterol.
Unlike simvastatin and pravastatin, atorvastatin is a completely synthetic compound.
It is currently being marketed by the pharmaceutical company Pfizer as Lipitor.
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Available forms
Atorvastatin is available as Lipitor in tablet form (10, 20, 40 or 80 mg) for oral administration. Tablets are white, elliptical, and film coated.
Mechanism of Action
Atorvastatin is a competitive inhibitor of HMG-CoA reductase. This enzyme catalyzes the reduction of 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, which is the rate limiting step in hepatic cholesterol synthesis.
Because cholesterol synthesis decreases, hepatic cells increase the number of LDL receptors on the surface of the cells, which increase the amount of LDL uptake by the hepatic cells, and decreases the amount of LDL in the blood.
Marketing
Reference: Drug Discovery Today editorial, 2005Template:Ref
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Sales, 2002-2004, as percentage of total during period.
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Sales, 2002-2004.
References
- Template:Note Maggon, Krishan. "Best-selling human medicines 2002-2004 (editorial)". 2005. Drug Discovery Today, 10(11):739-742.
- Lipitor: Prescribing Information. (http://www.lipitor.com/cwp/appmanager/lipitor/lipitorDesktop?_nfpb=true&_pageLabel=prescribingInformation) (2004) Pfizer Ireland Pharmaceuticals.
External links
- Manufacturer's site (http://www.lipitor.com) (lipitor.com)
- Frequently Asked Questions (http://www.duchs.com/information/Lipitor) Lipitor InformationTemplate:Statins