Pharm

Fluvastatin

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Fluvastatin, Lescol

  • 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. Fluvastatin is a preferred Statin if risk of significant Drug Interactions (fewer Drug Interactions)
  6. Fluvastatin 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. Fluvastatin 20 mg lowers LDL 17 to 22% (recommended starting dose)
  3. Fluvastatin 40 mg lowers LDL 23 to 25%
  4. Fluvastatin 80 mg lowers LDL 33 to 35%
  • Adverse Effects
  • Safety
  1. Pregnancy Category X
  2. Contraindicated in Lactation
  • Pharmacokinetics
  1. See Statin
  2. First-pass metabolism in all Statins except Pravastatin
  3. Protein binding
    1. As with most Statins (except Pravastatin), Fluvastatin is 90% Protein bound
  4. Cytochrome P450 Metabolism
    1. CYP3A4 isoenzyme metabolizes most Statins
    2. CYP2C9 isoenzyme metabolizes Fluvastatin
  • Dosing
  • Adults
  1. Specific LDL and HDL targets have been replaced with high-intensity Statin if 10 year Cardiovascular Risk >20%
  2. Low intensity Statin (age >75 years, or Statin intolerant)
    1. Fluvastatin 20-80 mg orally daily
  • Dosing
  • Child
  1. Approved for children over age 10 to 16 years old with Heterozygous familial Hyperlipidemia
  2. Start 20 mg orally daily
  3. Maximum: 80 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/organic anion transporting polypeptide inhibitors
    1. Cyclosporine (10-20 fold increase in Statin serum levels)
      1. Avoid with Fluvastatin
  3. CYP3A4/CYP2C9 Inhibitor
    1. Amiodarone
      1. Increased risk of Statin Myopathy (esp. with age >65, Obesity, renal or liver Impairment)
      2. Caution with Fluvastatin (consider dose adjustment)
    2. Warfarin (Increased INR and bleeding risk)
      1. Among the highest risk with Fluvastatin
  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. Caution with Fluvastatin
  5. CYP2C9 Inhibitor
    1. Fluconazole (Diflucan)
      1. Caution with Fluvastatin
  6. Other interactions
    1. Mibefradil (Posicor)
    2. Niacin
    3. Alcohol
      1. Increases risk of liver enzyme elevations