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Rosuvastatin

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Rosuvastatin, Crestor

  • See Also
  1. Hyperlipidemia
  2. Statin
  3. Statin-Induced Myopathy
  4. Atorvastatin
  5. Simvastatin
  6. Fluvastatin
  7. Lovastatin
  8. Pravastatin
  9. Pitavastatin
  • 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)
  • 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
  • Mechanism
  1. See Statin
  • 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%
  • Adverse Effects
  1. See Statin
  2. See Statin-Induced Myopathy
  • Safety
  1. Pregnancy Category X
  2. Contraindicated in Lactation
  • 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
  • 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)
  • 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
  • Monitoring
  1. See Statin
  2. Liver transaminase testing (AST,ALT) is no longer routinely indicated as of March 2012
  • 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
  • Resources
  1. See Statin
  2. Rosuvastatin (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ef243da2-d388-40e4-a1cb-a5e0688efc49
  • 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]