Rosuvastatin, a statin medication, used to prevent cardiovascular disease in those at high risk and treat abnormal lipids.
It is approved for the treatment of high LDL cholesterol (dyslipidemia), total cholesterol (hypercholesterolemia), and/or triglycerides (hypertriglyceridemia).
It is approved by the FDA for the primary prevention of cardiovascular events.
Trade name Crestor.
Approved for reducing risk of stroke, myocardial infarction, and revascularization procedures procedures and individuals with normal low density lipoprotein cholesterol levels and no clinically evident coronary heart disease but have increased risk based on age, high sensitivity C reactive protein levels and at least one additional cardiovascular disease risk factor.
Justification for the Use of Statins in Primary Prevention: an Intervention Trial Evaluating Rosustavastin (JUPITER) study demonstrated a 44% risk reduction in the primary endpoint in Rose’s status thatin Rosuvastatin 20 mg, compared with placebo.
R is recommended to be used together with dietary changes, exercise, and weight loss.
It is taken by mouth.
Pregnancy category AU: D
Bioavailability 20%.
Protein binding 88%.
Metabolism Liver: CYP2C9 (major) and CYP2C19-mediated; ~10% metabolized
Elimination half-life 19 hours
Excretion Feces (90%)
Use during pregnancy may harm the baby.
Coumarin anticoagulants
Cyclosporine
Colchicine
Drugs that may decrease the levels or activity of endogenous steroid hormones: cimetidine, ketoconazole, and spironolactone.
Medications for high cholesterol such as clofibrate, fenofibrate, gemfibrozil, and niacin.
Specific protease inhibitors.
Alcohol intake should be reduced while on rosuvastatin in order to decrease risk of developing liver damage.
Aluminum and magnesium hydroxide antacids should not be taken within two hours of taking rosuvastatin.
Coadministration of rosuvastatin with eluxadoline may increase the risk of rhabdomyolysis and myopathy.
It has structural similarities with most other synthetic statins.
Unlike other statins, rosuvastatin contains sulfur.
It works by inhibiting HMG-CoA reductase, an enzyme found in the liver that plays a role in producing cholesterol.
The primary use of rosuvastatin is for prevention of cardiovascular disease in those at high risk and the treatment of abnormal lipids.
Its effects on low-density lipoprotein (LDL) cholesterol are dose-related.
Higher doses are more efficacious in improving the lipid profile of patients with hypercholesterolemia than milligram-equivalent doses of atorvastatin and milligram-equivalent or higher doses of simvastatin and pravastatin.
It is able to modestly increase levels of high-density lipoprotein (HDL) cholesterol as well, as with other statins.
HDL increases by 7% with no dose effect noted.
Common side effects include:
abdominal pain, nausea, headaches, and muscle pains.
Serious side effects may include: rhabdomyolysis, liver problems, and diabetes.
Due to the potential of disrupting the infant’s lipid metabolism, patients should not breast feed while on rosuvastatin.
The risk of myopathy may be increased in Asian Americans: half the standard dose can have the same cholesterol-lowering benefit in those patients.
The risk of rhabdomyolysisis greater with than with other statins.
There isa 27% increase in investigator-reported diabetes mellitus in rosuvastatin-treated people.
Drugs with negative interactions with rosuvastatin:
The elimination half life is 19 hours and can be taken anytime night or day.