- See Hyperlipidemia Management for formal criteria
- See Statin
-
Hyperlipidemia
- Primary of vascular disease progression (e.g. CAD, CVA, DM, CKD, PAD)
- See Statin
- Rosuvastatin 5 mg lowers LDL 45%
- Rosuvastatin 10 mg lowers LDL: 46 to 52%
- Rosuvastatin 20 mg lowers LDL 50 to 55%
- Rosuvastatin 40 mg lowers LDL: 55 to 63%
- Pregnancy Category X
- Contraindicated in Lactation
- See Statin
- Undergoes first pass metabolism as with most Statins (except Pravastatin)
-
Protein binding
- As with most Statins (except Pravastatin), Rosuvastatin is 90% Protein bound
-
Cytochrome P450 Metabolism
- Rosuvastatin, like Pravastatin, is NOT metabolized by CYP3A4 isoenzyme
- Specific LDL and HDL targets have been replaced with high-intensity Statin if 10 year Cardiovascular Risk >20%
- High intensity Statin (age <75 years with 10 year Cardiovascular Risk >20%)
- Rosuvastatin 20-40 mg orally daily
- Low intensity Statin (age >75 years, or Statin intolerant)
- Rosuvastatin 25-10 mg orally daily
- Indications to start at lower dose (5 mg)
- Asians
- Higher drug levels leads to higher toxicity risk
- Renal Insufficiency (max 10 mg if CrCl < 30 ml/min)
- Hypothyroidism (uncontrolled)
- Age over 65 years
- Cyclosporine use (max dose 5 mg daily)
- Concurrent Gemfibrozil (max dose 10 mg daily)
- Heterozygous Familial Hyperlipidemia
- Age 8 to 9 years old
- Rosuvastatin 5 to 10 mg orally daily
- Age 10 years and older
- Rosuvastatin 5 to 20 mg orally daily
- Homozygous Familial Hyperlipidemia
- Age 7 to 17 years old
- Rosuvastatin 20 mg orally daily
- See Statin
-
Liver transaminase testing (AST,ALT) is no longer routinely indicated as of March 2012
-
Drug Interactions (See Contraindications above)
- See Statin
-
CYP3A4/organic anion transporting polypeptide inhibitors
- Cyclosporine (10-20 fold increase in Statin serum levels)
- Avoid with Rosuvastatin over 5 mg daily
- Macrolides (Erythromycin, Clarithromycin - 6-10 fold increase in Statin serum levels)
- Does not appear to significantly affect Rosuvastatin
- Azithromycin appears to be safe with Statins
- Protease inibitors (Atazanavir, Ritonavir, Lopinavir/Ritonavir)
- Avoid with Rosuvastatin over 10 mg daily
-
CYP3A4/CYP2C9 Inhibitor
- Warfarin (Increased INR and bleeding risk)
- Among the highest risk agents with Rosuvastatin
-
CYP2C9, CYP2C19/oragnic anion transporting polypeptide inhibitors
- Gemfibrozil (2-3 fold increase in Statin serum levels, >13 fold increase in Rhabdomyolysis risk)
- Avoid with Rosuvastatin over 10 mg daily
- Other interactions
- Mibefradil (Posicor)
- Niacin
- Alcohol
- Increases risk of liver enzyme elevations
loading