Pharm

Lovastatin

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Lovastatin, Mevacor, Altoprev

  • See Also
  1. Hyperlipidemia
  2. Statin
  3. Statin-Induced Myopathy
  4. Atorvastatin
  5. Rosuvastatin
  6. Simvastatin
  7. Fluvastatin
  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. Lovastatin 10 mg lowers LDL 21%
  3. Lovastatin 20 mg lowers LDL 24 to 29% (recommended starting dose)
  4. Lovastatin 40 mg lowers LDL 30 to 31%
  5. Lovastatin 80 mg lowers LDL 40 to 48%
  • 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), Lovastatin is 90% Protein bound
  4. Cytochrome P450 Metabolism
    1. CYP3A4 isoenzyme metabolizes most Statins, including Lovastatin
  • Dosing
  • Adult
  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. Lovastatin 20 to 40 mg orally daily (maximum 80 mg/day)
  • Dosing
  • Child
  1. Approved for children over age 10 to 17 years old with heterozygous Familial Hyperlipidemia
  2. Start 10 mg orally daily
  3. Maximum: 40 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 Lovastatin
    2. Calcium Channel Blocker
      1. Diltiazem (limit to 240 mg daily)
        1. Avoid with Lovastatin over 20 mg daily
      2. Verapamil (6-10 fold increase in Statin serum levels)
        1. Avoid with Lovastatin over 40 mg daily
    3. Grapefruit juice increases some Statin levels
      1. Lovastatin is among the drugs most affected
        1. Avoid with any Grapefruit juice (or minimal use)
      2. References
        1. (2016) Presc Lett 23(3):18
        2. Reamy (2007) Am Fam Physician 76:190-1 [PubMed]
  3. CYP3A4/organic anion transporting polypeptide inhibitors
    1. Cyclosporine (10-20 fold increase in Statin serum levels)
      1. Avoid with Lovastatin over 20 mg daily
    2. Macrolides (Erythromycin, Clarithromycin - 6-10 fold increase in Statin serum levels)
      1. Avoid while on Lovastatin (or stop Statin while on Macrolide)
      2. Azithromycin appears to be safe with Statins
    3. Protease inibitors (Atazanavir, Ritonavir, Lopinavir/Ritonavir)
      1. Avoid with Lovastatin
  4. CYP3A4/CYP2C9 Inhibitor
    1. Amiodarone
      1. Increased risk of Statin Myopathy (esp. with age >65, Obesity, renal or liver Impairment)
      2. Avoid with Lovastatin over 40 mg daily
    2. Warfarin (Increased INR and bleeding risk)
      1. Among the highest risk with Lovastatin
  5. 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 Lovastatin over 20 mg daily
  6. Other interactions
    1. Mibefradil (Posicor)
    2. Niacin
    3. Alcohol
      1. Increases risk of liver enzyme elevations
  • Resources
  1. See Statin
  2. Lovastatin Extended Release (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=8c0db100-5df9-49c3-8af9-1bc03ae609b9
  3. Lovastatin Regular Release (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=5c707089-fb5b-4016-8ca7-11bbcfb57854
  • 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]