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Pathway Description
Rosuvastatin Action Pathway
Homo sapiens
Drug Action Pathway
Rosuvastatin, sold as Crestor, Rosulip and Zuvamor, belongs to the class of drugs known as statins. It is taken orally to inhibit the endogenous production of cholesterol in the liver. Statins do this by inhibiting the enzyme 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. This enzyme is typically responsible for the conversion of HMG-CoA to mevalonic acid, the third and rate-limiting step of cholesterol, LDL and VLDL synthesis. Rosuvastatin has a similar structure to 3-hydroxy-3-methylglutaryl-CoA, and acts to competitively inhibit the action of HMG-CoA reductase.
Statins such as rosuvastatin are used to lower the risk of cardiovascular disease due to higher than normal levels of LDL ad VLDL, which are sometimes known as bad cholesterol. Cardiovascular disease can include heart attacks, angina, strokes and artery disease, and LDL and VLDL levels are a risk factor for its development. Because rosuvastatin is not highly metabolized by Cytochrome P450 enzymes and is taken up quickly due to its hydrophilicity, it has less drug interactions than other statins. It is also the most potent statin, meaning a smaller dose is required. However, it does not prevent CVD any better than other statins.
References
Rosuvastatin Pathway References
Crestor. (2009). e-CPS (online version of Compendium of Pharmaceuticals and Specialties). Retrieved June 30, 2009.
Reszka AA, Rodan GA: Bisphosphonate mechanism of action. Curr Rheumatol Rep. 2003 Feb;5(1):65-74.
Pubmed: 12590887
Schmidt, E.B., & Larsen, M.L. HMG-CoA-reductase-inhibitors. In S. Offermanns, & W. Rosenthal (Eds.). Encyclopedic reference of molecular pharmacology (2004);p. 460-463. Berlin, Germany: Springer.
Steroid Biosynthesis References
Lehninger, A.L. Lehninger principles of biochemistry (4th ed.) (2005). New York: W.H Freeman.
Norman, A.W, and Litwack, G. Hormones (2nd ed.) (1997) San Diego : Academic Press.
Salway, J.G. Metabolism at a glance (3rd ed.) (2004). Alden, Mass.: Blackwell Pub.
Vance, D.E., and Vance, J.E. Biochemistry of lipids, lipoproteins, and membranes (4th ed.) (2002) Amsterdam; Boston: Elsevier.
Simons J: The $10 billion pill. Fortune. 2003 Jan 20;147(1):58-62, 66, 68.
Pubmed: 12602122
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