II. Indications

  1. See Hyperlipidemia Management for formal criteria
  2. See Statin
  3. Hyperlipidemia
  4. Primary of vascular disease progression (e.g. CAD, CVA, DM, CKD, PAD)

III. Contraindications

  1. See Statin
  2. Drug Interactions
    1. See Statin regarding Myopathy and hepatitis risk
  3. Pregnancy (Teratogen)
  4. Acute Liver Failure or decompensated Cirrhosis

IV. Mechanism

  1. See Statin

V. Efficacy

  1. See Statin
  2. Rosuvastatin 5 mg lowers LDL 45%
  3. Rosuvastatin 10 mg lowers LDL: 46 to 52%
  4. Rosuvastatin 20 mg lowers LDL 50 to 55%
  5. Rosuvastatin 40 mg lowers LDL: 55 to 63%

VI. Adverse Effects

VII. Safety

  1. Pregnancy Category X
  2. Contraindicated in Lactation

VIII. Pharmacokinetics

  1. See Statin
  2. Undergoes first pass metabolism as with most Statins (except Pravastatin)
  3. Protein binding
    1. As with most Statins (except Pravastatin), Rosuvastatin is 90% Protein bound
  4. Cytochrome P450 Metabolism
    1. Rosuvastatin, like Pravastatin, is NOT metabolized by CYP3A4 isoenzyme

IX. Dosing: Adult

  1. Specific LDL and HDL targets have been replaced with high-intensity Statin if 10 year Cardiovascular Risk >20%
  2. High intensity Statin (age <75 years with 10 year Cardiovascular Risk >20%)
    1. Rosuvastatin 20-40 mg orally daily
  3. Low intensity Statin (age >75 years, or Statin intolerant)
    1. Rosuvastatin 25-10 mg orally daily
  4. Indications to start at lower dose (5 mg)
    1. Asians
      1. Higher drug levels leads to higher toxicity risk
    2. Renal Insufficiency (max 10 mg if CrCl < 30 ml/min)
    3. Hypothyroidism (uncontrolled)
    4. Age over 65 years
    5. Cyclosporine use (max dose 5 mg daily)
    6. Concurrent Gemfibrozil (max dose 10 mg daily)

X. Dosing: Child

  1. Heterozygous Familial Hyperlipidemia
    1. Age 8 to 9 years old
      1. Rosuvastatin 5 to 10 mg orally daily
    2. Age 10 years and older
      1. Rosuvastatin 5 to 20 mg orally daily
  2. Homozygous Familial Hyperlipidemia
    1. Age 7 to 17 years old
      1. Rosuvastatin 20 mg orally daily

XI. Monitoring

  1. See Statin
  2. Liver transaminase testing (AST,ALT) is no longer routinely indicated as of March 2012

XII. Drug Interactions (See Contraindications above)

  1. See Statin
  2. CYP3A4/organic anion transporting polypeptide inhibitors
    1. Cyclosporine (10-20 fold increase in Statin serum levels)
      1. Avoid with Rosuvastatin over 5 mg daily
    2. Macrolides (Erythromycin, Clarithromycin - 6-10 fold increase in Statin serum levels)
      1. Does not appear to significantly affect Rosuvastatin
      2. Azithromycin appears to be safe with Statins
    3. Protease inibitors (Atazanavir, Ritonavir, Lopinavir/Ritonavir)
      1. Avoid with Rosuvastatin over 10 mg daily
  3. CYP3A4/CYP2C9 Inhibitor
    1. Warfarin (Increased INR and bleeding risk)
      1. Among the highest risk agents with Rosuvastatin
  4. CYP2C9, CYP2C19/oragnic anion transporting polypeptide inhibitors
    1. Gemfibrozil (2-3 fold increase in Statin serum levels, >13 fold increase in Rhabdomyolysis risk)
      1. Avoid with Rosuvastatin over 10 mg daily
  5. Other interactions
    1. Mibefradil (Posicor)
    2. Niacin
    3. Alcohol
      1. Increases risk of liver enzyme elevations

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Related Studies

Cost: Medications

rosuvastatin (on 12/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
ROSUVASTATIN CALCIUM 10 MG TAB Generic $0.05 each
ROSUVASTATIN CALCIUM 20 MG TAB Generic $0.08 each
ROSUVASTATIN CALCIUM 40 MG TAB Generic $0.12 each
ROSUVASTATIN CALCIUM 5 MG TAB Generic $0.05 each
crestor (on 9/21/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
CRESTOR 10 MG TABLET Generic $0.05 each
CRESTOR 20 MG TABLET Generic $0.08 each
CRESTOR 40 MG TABLET Generic $0.12 each
CRESTOR 5 MG TABLET Generic $0.05 each

Ontology: rosuvastatin (C0965129)

Definition (NCI) A statin with antilipidemic and potential antineoplastic activities. Rosuvastatin selectively and competitively binds to and inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a precursor of cholesterol. This leads to a decrease in hepatic cholesterol levels and increase in uptake of LDL cholesterol. In addition, rosuvastatin, like other statins, exhibits pro-apoptotic, growth inhibitory, and pro-differentiation activities in a variety of tumor cell types; these antineoplastic activities may be due, in part, to inhibition of the isoprenylation of Ras and Rho GTPases and related signaling cascades.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C422923
SnomedCT 700067006, 406436002
LNC LP171638-2
English rosuvastatin [Chemical/Ingredient], rosuvastatin, Rosuvastatin (substance), ROSUVASTATIN, 6-Heptenoic acid, 7-(4-(4-fluorophenyl)-6-(1-methylethyl)-2-(ethyl(methylsulfonyl)amino)-5-pyrimidinyl)-3,5-dihydroxy-, (3R,5S,6E), Rosuvastatin, Rosuvastatin (product)
Spanish rosuvastatina (producto), rosuvastatina

Ontology: Rosuvastatin calcium (C1101751)

Definition (NCI) The calcium salt form of rosuvastatin, a statin with antilipidemic activity. Rosuvastatin selectively and competitively binds to and inhibits hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, the enzyme which catalyzes the conversion of HMG-CoA to mevalonate, a precursor of cholesterol. This leads to a decrease in hepatic cholesterol levels and increase in uptake of LDL cholesterol.
Definition (NCI_NCI-GLOSS) A drug used to lower the amount of cholesterol and other harmful substances, such as triglycerides, in the blood. It is also being studied in the prevention and treatment of some types of cancer and other conditions. Crestor blocks an enzyme that helps make cholesterol in the body and it helps break down cholesterol. It also may cause cancer cells to die and may inhibit the growth of blood vessels that cancer cells need to grow. It is a type of HMG-CoA reductase inhibitor and a type of statin.
Concepts Biologically Active Substance (T123) , Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C422923
SnomedCT 406435003
English HMG-CoA reductase inhibitors rosuvastatin calcium, rosuvastatin calcium (medication), ROSUVASTATIN CALCIUM, Rosuvastatin calcium (substance), Rosuvastatin calcium, rosuvastatin calcium, Rosuvastatin Calcium
Spanish rosuvastatina cálcica (sustancia), rosuvastatina cálcica