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Atorvastatin - cholesterol control

On WHO Model List of Essential Medicines : NO

Alternative names: Lipitor, Atorva

 

Atorvastatin, marketed under the trade name Lipitor among others, is a member of the drug class known as statins or HMG CoA reductase inhibitors. Atorvastatin was discovered by Bruce Roth in 1985 and reduces levels of "bad" cholesterol (low-density lipoprotein, or LDL) and triglycerides in the blood, while increasing levels of "good" cholesterol (high-density lipoprotein, or HDL).

It works by reducing the amount of cholesterol made by the liver - like all statins, atorvastatin competitively inhibits HMG-CoA reductase, an enzyme found in liver tissue that plays a key role in production of cholesterol in the body. Statins in general have a similar structure to HMG-CoA and will fit on the enzyme’s active site and compete with the natural reactor. This competition reduces the molecular pathway that leads to the production of cholesterol.

In rabbits, statins also increase LDL uptake. The liver cells sense the reduced levels of liver cholesterol and seek to compensate by synthesizing LDL receptors that bind to passing LDL which draws cholesterol out of the circulation. The cholesterol is then reprocessed into bile salts. All in all, statins lower cholesterol levels by decreasing their production and increasing their uptake.

 Atorvastatin is used along with a proper diet to help treat high cholesterol, and to lower the risk of stroke, heart attack, or other heart complications in people with type 2 diabetes, coronary heart disease, or other risk factors.

Although atorvastatin was the fifth drug in the class of statins to be developed, clinical trials showed that atorvastatin caused a more dramatic reduction of bad cholesterol than the other statin drugs. From 1996 to 2012 under the trade name Lipitor, atorvastatin became the world's best-selling drug of all time, with more than US$125 billion in sales over approximately 14.5 years.

 

Toxicology report

http://www.fda.gov/ohrms/dockets/ac/03/briefing/3968B1_02_F-FDA-PharmTox%20Review.doc

http://www.biomedcentral.com/2050-6511/14/15

http://www.ncbi.nlm.nih.gov/pubmed/8864188


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