What is rosuvastatin, and how does it work (mechanism of action)?

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

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.

What brand names are available for rosuvastatin?

Crestor

Is rosuvastatin available as a generic drug?

GENERIC AVAILABLE: No

Do I need a prescription for rosuvastatin?

Yes

What are the uses for rosuvastatin?

Rosuvastatin is used for the reduction of blood total cholesterol, HDL cholesterol and triglyceride levels, and to increase HDL cholesterol levels. Rosuvastatin also is used for reducing the risk of heart attacks, stroke, and arterial revascularization procedures in patients without clinically evident coronary heart disease but with multiple risk factors for heart disease.

What are the side effects of rosuvastatin?

The most common side effects of rosuvastatin are:

Other important side effects include:

Symptoms may start one day to years after starting treatment and resolve within a median of three weeks after stopping the statin.

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What is the dosage for rosuvastatin?

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.

Which drugs or supplements interact with rosuvastatin?

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 (Lopid) or other drugs that may cause liver or muscle injury may increase the incidence of the muscle injury.

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Is rosuvastatin safe to take if I’m pregnant or breastfeeding?

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.

What else should I know about rosuvastatin?

What preparations of rosuvastatin are available?

Tablets: 5, 10, 20, and 40 mg

How should I keep rosuvastatin stored?

Rosuvastatin should be stored at room temperature between 2 C – 25 C (36 F – 77 F).

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Medically Reviewed on 3/1/2019

References

Medically reviewed by John P. Cunha, DO, FACOEP; Board Certified Emergency Medicine

REFERENCE:

FDA Prescribing Information