Rosuvastatin

Aka: Rosuvastatin, Crestor

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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

  1. See Statin
  2. See Statin-Induced Myopathy

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

XIII. Resources

  1. See Statin
  2. Rosuvastatin (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ef243da2-d388-40e4-a1cb-a5e0688efc49

XIV. References

  1. (2017) Presc Lett 24(11): 62
  2. (2012) Presc Lett 19(5): 25
  3. (2012) Presc Lett, Characteristics of Various Statins, #280502
  4. Carpenter (2019) Am Fam Physician 99(9):558-64 [PubMed]
  5. Chong (2001) Am J Med 111:390-400 [PubMed]
  6. Crouch (2001) Am Fam Physician 63(2):309-20 [PubMed]
  7. Gillett (2011) Am Fam Physician 83(6): 711-6 [PubMed]
  8. Jones (1998) Am J Cardiol 81:582-7 [PubMed]
  9. Sasaki (1998) Clin Ther 20:539-48 [PubMed]

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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
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information. GoodRx is another tool for finding lower drug prices.

Related Topics in Pharmacology

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