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Crestor (rosuvastatin calcium)


HMG-CoA reductase inhibitor (statin)




Adjunct to diet to decrease total cholesterol, LDL, apolipoprotein B, and TG levels, and to increase HDL levels in primary hyperlipidemia or mixed dyslipidemia, hypertriglyceridemia, primary dysbetalipoproteinemia, heterozygous familial hypercholesterolemia (HeFH) (adolescent boys and girls, who are at least 1 yr postmenarche, 10-17 yrs of age), homozygous familial hypercholesterolemia (HoFH), slow progression of atherosclerosis, and for prevention of cardiovascular disease.



Hyperlipidemia and Mixed Dyslipidemia/Hypertriglyceridemia/Primary Dysbetalipoproteinemia (Type III Hyperlipoproteinemia)/Slowing of the Progression of Atherosclerosis:

General Dose:
Initial: 10-20mg qd
Range: 5-40mg qd

When initiating treatment or switching from another HMG-CoA reductase inhibitor, use the appropriate starting dose 1st, then titrate according to patient's response and individualized goal of therapy

Analyze lipid levels w/in 2-4 weeks and adjust dose accordingly

Use 40mg dose only if LDL goal is not achieved w/ 20mg dose

Homozygous Familial Hypercholesterolemia

Initial: 20mg qd

Prevention of Cardiovascular Disease

Reduce the risk of stroke, MI, arterial revascularization procedures in patients w/o clinically evident coronary heart disease but w/ an increased risk of cardiovascular disease (CVD) based on age (men ≥50 yrs of age and women ≥60 yrs of age), hsCRP ≥2mg/L, and the presence of at least 1 additional CVD risk factor


Heterozygous Familial Hypercholesterolemia

10-17 Years (At Least 1-Year Postmenarche):
Individualize dose
Usual: 5-20mg/day
Titrate: Adjust dose at intervals of ≥4 weeks
Max: 20mg/day


Concomitant Medications
5mg qd
Atazanavir/Ritonavir or Lopinavir/Ritonavir or Simeprevir or Gemfibrozil:
5mg qd
10mg qd

Renal Impairment
Severe (CrCl <30mL/min) Not on Hemodialysis:
Initial: 5mg qd
Max: 10mg qd

Hepatic Impairment
Chronic Alcohol Liver Disease: Use w/ caution

Other Important Considerations
Asian Patients:
Initial: 5mg qd


Oral route

Take at any time of day, w/ or w/o food
Swallow tab whole
Do not take 2 doses w/in 12 hrs of each other


Tab: 5mg, 10mg, 20mg, 40mg


Active liver disease including unexplained persistent elevations of hepatic transaminase levels, women who are pregnant or may become pregnant, nursing mothers.


Myopathy (including immune-mediated necrotizing myopathy [IMNM]) and rhabdomyolysis reported w/ increased risk at 40mg; caution in patients w/ predisposing factors for myopathy (eg, age ≥65 yrs, inadequately treated hypothyroidism, renal impairment). D/C if markedly elevated CPK levels occur or myopathy is diagnosed or suspected. Temporarily withhold in any patient w/ an acute, serious condition suggestive of myopathy or predisposing to the development of renal failure secondary to rhabdomyolysis. Increases in serum transaminases reported. Fatal and nonfatal hepatic failure reported (rare); promptly interrupt therapy if serious liver injury w/ clinical symptoms and/or hyperbilirubinemia or jaundice occurs, and do not restart if no alternate etiology is found. Caution in patients who consume substantial quantities of alcohol and/or have a history of chronic liver disease, or in elderly. Dipstick-positive proteinuria and microscopic hematuria reported; consider dose reduction for patients w/ unexplained persistent proteinuria and/or hematuria. Increases in HbA1c and FPG levels reported.


Headache, myalgia, nausea, dizziness, arthralgia, constipation, asthenia, abdominal pain.


See Dose Modification. Cyclosporine, gemfibrozil, lopinavir/ritonavir, atazanavir/ritonavir, and simeprevir may increase levels. Increased risk of myopathy w/ some other lipid-lowering therapies (fibrates or niacin), gemfibrozil, cyclosporine, lopinavir/ritonavir, atazanavir/ritonavir, or simeprevir. Avoid w/ gemfibrozil. Caution w/ coumarin anticoagulants. May enhance the risk of skeletal muscle effects w/ ≥1g/day of niacin. Caution w/ drugs that may decrease levels or activity of endogenous steroid hormones (eg, ketoconazole, spironolactone, cimetidine), fenofibrates, or protease inhibitors. Caution w/ colchicine; cases of myopathy, including rhabdomyolysis, reported.


Category X, not for use in nursing.


HMG-CoA reductase inhibitor; produces lipid-modifying effects by increasing the number of hepatic LDL receptors on the cell surface to enhance uptake and catabolism of LDL and by inhibiting hepatic synthesis of VLDL, which reduces the total number of VLDL and LDL particles.


Absorption: Absolute bioavailability (20%); Tmax=3-5 hrs. Distribution: Vd=134L; plasma protein binding (88%). Metabolism: CYP2C9; N-desmethyl rosuvastatin (major metabolite). Elimination: Feces (90%); T1/2=19 hrs.


Assess for active liver disease (including chronic alcohol liver disease), unexplained persistent elevations in serum transaminases, risk factors for developing myopathy or rhabdomyolysis, pregnancy/nursing status, and possible drug interactions. Obtain baseline lipid profile, LFTs, and evaluate renal function. Check INR w/ coumarin anticoagulants.


Monitor for signs/symptoms of myopathy (including IMNM), rhabdomyolysis, endocrine dysfunction, proteinuria, hematuria, and other adverse reactions. Monitor lipid levels, CPK, and LFTs. Monitor INR w/ coumarin anticoagulants frequently during early therapy.


Advise to report promptly any unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever or if muscle signs/symptoms persist after discontinuing therapy. Advise to wait at least 2 hrs if taking an antacid containing a combination of aluminum and magnesium hydroxide. Inform of potential hazard to fetus if patient becomes pregnant while on therapy. Advise to promptly report any symptoms that may indicate liver injury (eg, fatigue, anorexia, right upper abdominal discomfort, dark urine, jaundice).


20-25°C (68-77°F). Protect from moisture.


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