- Atorvastatin was first synthesized in 1985 by Bruce Roth while working at Parke-Davis Warner-Lambert Company (now Pfizer).
- With sales of US$12.4 billion, Atorvastatin (Lipitor) was the top-selling branded pharmaceutical in the world.
U.S. patent protection is scheduled to expire in June 2011. However, Pfizer made an agreement with Ranbaxy Laboratories to delay the generic launch in the U.S. until November 2011.
- It is sold in India under the trade name Atarvadel
- It is a member of the drug class known as statins, used for lowering blood cholesterol. It also stabilizes plaque and prevents strokes through anti-inflammatory and other mechanisms. Like all statins, atorvastatin works by inhibiting HMG-CoA reductase, an enzyme found in liver tissue that plays a key role in production of cholesterol in the body.
Machanism of Action:-
As with other statins, atorvastatin is a competitive inhibitor of HMG-CoA reductase. Unlike most others, however, it is a completely synthetic compound. HMG-CoA reductase catalyzes the reduction of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate, which is the rate-limiting step in hepatic cholesterol biosynthesis. Inhibition of the enzyme decreases de novo cholesterol synthesis, increasing expression of low-density lipoprotein receptors (LDL receptors) on hepatocytes. This increases LDL uptake by the hepatocytes, decreasing the amount of LDL-cholesterol in the blood. Like other statins, atorvastatin also reduces blood levels of triglycerides and slightly increases levels of HDL-cholesterol.
In clinical trials, drugs that block cholesterol uptake like ezetimibe combine with and complement those that block biosynthesis like atorvastatin or simvastatin in lowering cholesterol or targeting levels of LDL.
Atorvastatin calcium tablets are marketed by Pfizer under the trade name Lipitor, in tablets (10, 20, 40 or 80 mg) for oral administration. Tablets are white, elliptical, and film-coated. Pfizer also packages the drug in combination with other drugs, such as with Caduet. Pfizer recommends that patients do not break tablets in half to take half-doses, even when this is recommended by their doctors.
Atorvastatin calcium is made in tablet form by generic drug makers under various brand names as :-
The primary uses of atorvastatin is for the treatment of dyslipidemia and the prevention of cardiovascular disease.
- Hypercholesterolemia and mixed dyslipidemia to reduce total cholesterol, as well as increase HDL levels
- Heterozygous familial hypercholesterolemia in pediatric patients
- Homozygous familial hypercholesterolemia
- Primary dysbetalipoproteinemia
- Combined hyperlipidemia
Secondary prevention in people with coronary heart disease and multiple risk factors for myocardial infarction, stroke, unstable angina, and revascularization
Myocardial infarction and stroke prophylaxis in patients with type II diabetes
Concomitant therapy considerations: may be used in combination with bile acid resins. It is not recommended to combine statin treatment with fibrates because of the increased risk of myopathy related adverse reactions. Drug dose must be lowered in Hepatic insufficiency.
More information about Lipitor & Atorvastatin will be explored in our next posts