Medications and Drugs

Pharmacy Author: Omudhome Ogbru, Pharm.D.
Medical Editor: Jay Marks, M.D.

GENERIC NAME: rosuvastatin

BRAND NAME: Crestor

DRUG CLASS AND MECHANISM: Rosuvastatin is an oral drug for lowering blood cholesterol levels. It belongs to a class of drugs called HMG-CoA reductase inhibitors, more commonly referred to as "statins". Other drugs in this class include simvastatin (Zocor), lovastatin (Mevacor), pravastatin (Pravachol), atorvastatin (Lipitor) and fluvastatin (Lescol). These drugs reduce cholesterol levels by inhibiting HMG-CoA reductase, an enzyme that produces cholesterol in the liver. Rosuvastatin and other statins lower blood total cholesterol as well as blood LDL cholesterol levels. LDL cholesterol is the "bad" type of cholesterol that increases the risk of coronary artery disease (atherosclerosis) and heart attacks. Lowering LDL cholesterol levels slows the progression of coronary artery disease and may even reverse it. Statins also increase HDL cholesterol, the "good" type of cholesterol, and reduce triglycerides.

Scientists have discovered that in addition to atherosclerosis, inflammation of the coronary arteries may also contribute to the development of heart attacks. The presence of inflammation can be determined by measuring a chemical in the blood called highly sensitive C-reactive protein (Hs-CRP). Moreover, Hs-CRP can be used to predict the occurrence of heart attacks, strokes and death. Hs-CRP is, in fact, a better predictor of the risk for heart attacks than LDL cholesterol. Scientists have found that statins reduce the level of Hs-CRP in the body, presumably by reducing inflammation in the coronary arteries, and this may be another mechanism through which statins prevent heart attacks, strokes, and death. More research needs to be conducted, however, to confirm the importance of inflammation and the mechanisms through which statins work. Rosuvastatin was approved by the FDA in August 2003.

PRESCRIPTION: Yes

GENERIC AVAILABLE: No

PREPARATIONS: Tablets: 5, 10, 20, 40 mg

STORAGE: Store at room temperature between 2-25 C (36-77 F).

PRESCRIBED FOR: Rosuvastatin is used for the reduction of blood total cholesterol, HDL cholesterol and triglyceride levels and to increase HDL cholesterol levels.

DOSING: The starting dose for most adults is 5 mg once daily. The maximum dose is 40 mg daily, and this dose should be reserved for patients who do not adequately respond to a 20 mg dose.

DRUG INTERACTIONS: When administered with cyclosporine, the blood level of rosuvastatin increases seven fold, and this could increase the side effects of rosuvastatin.

Rosuvastatin increases the action of the blood thinner warfarin (Coumadin) and could increase the risk of bleeding from warfarin. Antacids reduce the absorption of rosuvastatin and should be administered two hours after rosuvastatin. The use of rosuvastatin with nicotinic acid, gemfibrozil or other drugs that may cause liver or muscle injury may increase the incidence of the muscle injury.

PREGNANCY: Statins should not be used by pregnant women because there is a high risk of harm to the fetus.

Report Problems to the Food and Drug Administration   You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.

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