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 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.

NURSING MOTHERS: There is no information on whether rosuvastatin is excreted in breast milk.

SIDE EFFECTS: The most common side effects of rosuvastatin are headache, nausea, vomiting, diarrhea and muscle pain. The most serious side effects are liver failure, muscle breakdown (rhabdomyolysis) and kidney failure. Liver failure caused by statins is very rare. More often, statins cause increases in liver tests due to injury to the liver. The test levels usually return to normal with continued therapy, but if the level is over three times the upper limit of normal or baseline, practitioners usually stop the statin. Periodic measurement of liver tests is recommended for all statins. For rosuvastatin, these tests should be obtained before therapy is started, twelve weeks after therapy is started, when the dose is increased, if there is a medical concern, and periodically during prolonged treatment. Rhabdomyolysis is a very rare but serious side effect of statin therapy. When used alone the frequency of rhabdomyolysis due to statins is less than one percent. Rhabdomyolysis is a process in which there is severe injury to muscles leading to severe pain and the release of muscle protein (myoglobin) into the blood. Myoglobin may cause kidney failure. To prevent the occurrence of rhabdomyolysis, patients taking statins who develop unexplained muscle pain, weakness or tenderness should report the symptoms to their provider. Rosuvastatin may cause reversible increases in the amount of protein excreted by the kidneys, and in some patients kidney failure has occurred as a result. This effect depends on the dose and occurs more often at the 40 mg dose.

Last Editorial Review: 10/22/2003 9:51:01 PM

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