Pharm

Atorvastatin

search

Atorvastatin, Lipitor

  • 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)
  5. Atorvastatin is a preferred Statin in Renal Insufficiency
  • 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. Atorvastatin 10 mg lowers LDL 38% (recommended starting dose)
  3. Atorvastatin 20 mg lowers LDL 43 to 46%
  4. Atorvastatin 40 mg lowers LDL 50 to 51%
  5. Atorvastatin 80 mg lowers LDL 54 to 60%
  6. Triglycerides lowered 40%
  • Adverse Effects
  • 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), Atorvastatin is 90% Protein bound
  4. Cytochrome P450 Metabolism
    1. CYP3A4 isoenzyme metabolizes most Statins, including Atorvastatin
  • Dosing
  • Adults
  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. Atorvastatin 40-80 mg orally daily
  3. Low intensity Statin (age >75 years, or Statin intolerant)
    1. Atorvastatin 10-20 mg orally daily
  • Dosing
  • Children
  1. May use in age 10 years old and older
  2. Start 10 mg orally daily
  3. Maximum: 20 mg/day
  • 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 Inhibitors
    1. Azole Antifungals (Intraconazole, Ketoconazole - 10-20 fold increase in Statin serum levels)
      1. Increased risk of Statin Myopathy (esp. with age >65, Obesity, renal or liver Impairment)
      2. Avoid with Atorvastatin over 20 mg daily
    2. Calcium Channel Blocker
      1. Diltiazem (limit to 240 mg daily)
        1. Remain alert for Statin Myopathy with Atorvastatin
      2. Verapamil (6-10 fold increase in Statin serum levels)
        1. Remain alert for Statin Myopathy with Atorvastatin
    3. Grapefruit juice increases some Statin levels
      1. Drugs affected moderately: Atorvastatin
        1. Limit Grapefruit juice to 8-16 ounces daily (effects more likely to manifest at 32 ounces)
        2. Limit juice timing to opposite Statin dose
          1. Take juice at night, if Statin taken in morning
  3. CYP3A4/organic anion transporting polypeptide inhibitors
    1. Cyclosporine (10-20 fold increase in Statin serum levels)
      1. Avoid with Atorvastatin over 10 mg daily
    2. Macrolides (Erythromycin, Clarithromycin - 6-10 fold increase in Statin serum levels)
      1. Avoid with Atorvastatin over 20 mg daily
      2. Azithromycin appears to be safe with Statins
    3. Protease inibitors (Atazanavir, Ritonavir, Lopinavir/Ritonavir)
      1. Avoid with Atorvastatin over 20 mg daily
  4. CYP3A4/CYP2C9 Inhibitor
    1. Amiodarone
      1. Increased risk of Statin Myopathy (esp. with age >65, Obesity, renal or liver Impairment)
      2. Caution with Atorvastatin (consider dose adjustment)
    2. Warfarin (Increased INR and bleeding risk)
      1. Lower risk with Atorvastatin (compared with other Statins)
  5. CYP2C9, CYP2C19/oragnic anion transporting polypeptide inhibitors
  6. Other interactions
    1. Mibefradil (Posicor)
    2. Niacin
    3. Alcohol
      1. Increases risk of liver enzyme elevations