Atorvastatin

Atorvastatin chemical structure
Atorvastatin

[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.

Contents

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

Missing image
Piechart_sales_2002-2004.png
Sales, 2002-2004, as percentage of total during period.

Missing image
Line_chart_sales_2002-2004.png
Sales, 2002-2004.

References

  1. Template:Note Maggon, Krishan. "Best-selling human medicines 2002-2004 (editorial)". 2005. Drug Discovery Today, 10(11):739-742.
  2. Lipitor: Prescribing Information. (http://www.lipitor.com/cwp/appmanager/lipitor/lipitorDesktop?_nfpb=true&_pageLabel=prescribingInformation) (2004) Pfizer Ireland Pharmaceuticals.

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