Atorvastatin

Pharmacologic class

HMG-CoA reductase inhibitor (statin)

Lipitor (as calcium salt)

As an adjunct to diet in high cholesterol and inherited imbalances of cholesterol, and in the treatment of elevated serum triglycerides.

Reduces cholesterol production by the liver by acting as a competitive inhibitor of HMG CoA reductase, which catalyzes the rate-limiting step in cholesterol biosynthesis within the liver. Statins occupy a portion of the binding site of HMG CoA, and block access to the active site on the enzyme.

Active liver disease, unexplained persistent elevated serum transaminases, pregnancy (Category X), nursing mothers.

Avoid using gemfibrozil, clofibrate, fibric acid derivatives, erythromycin, nicotinic acid, or azole antifungals at the same time. Has some additive effects with colestipol, and dosing should be separated by at least four hours. Atorvastatin may increase the serum levels of digoxin and oral contraceptives. Patients should be monitored for myopathy if taking immunosuppressants such as cyclosporine. Take caution with any drug that decreases levels or activity of steroid hormones such as ketoconazole, spironolactone, or cimetidine.

GI upset, headache, muscle aches, joint aches, rash, elevated liver enzymes, myopathy, muscle breakdown with kidney dysfunction.

Atorvastatin may reduce the proliferation of smooth muscle cells and act as an antioxidant and an anti-inflammatory, reducing heart attacks and other vascular events.

August 3, 2002

http://www.uptodate.com/patient_info/topicpages/topics/36288D0.asp

http://www.fpnotebook.com/CV212.htm