PREPARATIONS: Tablets: 5, 10, 20, and 40 mg
DRUG INTERACTIONS: When administered with cyclosporine, the blood level of rosuvastatin increases seven fold, and this could increase the side effects of rosuvastatin.
Antacids reduce the absorption of rosuvastatin and should be administered two hours after rosuvastatin.
PREGNANCY AND BREASTFEEDING SAFETY: Statins should not be used by pregnant women because there is a high risk of harm to the fetus.
There is no information on whether rosuvastatin is excreted in human milk.
STORAGE: Rosuvastatin should be stored at room temperature between 2 C - 25 C (36 F - 77 F).
DOSAGE: 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 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.
Medically reviewed by Eni Williams, PharmD, PhD
Reference: FDA Prescribing Information
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