Atorvastatin chemical structure
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Lipitor


Atorvastatin (INN) (IPA: ) is a member of the drug class known as 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. more...

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Unlike most statins, atorvastatin is a completely synthetic compound.

Atorvastatin is currently marketed by the pharmaceutical company Pfizer as Lipitor®. In some countries it may also be known as: Sortis®, Torvast®, Totalip®, or Xarator®. With 2004 sales of US$10.9 billion, it is the best selling drug in the world.

Clinical use

Indications

Atorvastatin is indicated as an adjunct to diet for the treatment of dyslipidaemia, specifically hypercholesterolaemia. It has also been used in the treatment of mixed hyperlipidaemia. (Rossi, 2006)

Available forms

Atorvastatin is marketed as atorvastatin calcium under the trade name Lipitor, in tablets (10, 20, 40 or 80 mg) for oral administration. Tablets are white, elliptical, and film coated.

Adverse effects

Common adverse drug reactions (ADRs) associated with atorvastatin therapy include: myalgia, mild transient gastrointestinal symptoms, elevated hepatic transaminase concentrations, headache, insomnia, and/or dizziness. (Rossi, 2006)

Myopathy and rhabdomyolysis are rare, but serious, dose-related ADRs associated with statin therapy. Risk is increased in patients with renal impairment, serious concurrent illness; and/or concomitant use of drugs which inhibit CYP3A4. (Rossi, 2006)

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.

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Pfizer and Ranbaxy Laboratories went to court last month over the industry's No. 1 pharmaceutical Lipitor
From Drug Store News, 12/13/04 by James Frederick

Generics News--Pfizer and Ranbaxy Laboratories went to court last month over the industry's No. 1 pharmaceutical Lipitor. Ranbaxy is the first to challenge two of Pfizer's Lipitor patents, which are supposed to protect the statin from generic competition until at least 2009.

Ranbaxy's chances of prevailing in this case are slim, many analysts are saying, but the potential upside for Ranbaxy is tremendous. Lipitor generated $7.4 billion in U.S. sales for the 12 months ending September, according to IMS Health data.

COPYRIGHT 2004 Reproduced with permission of the copyright holder. Further reproduction or distribution is prohibited without permission.
COPYRIGHT 2005 Gale Group

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