Pharm

Zileuton

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Zileuton, Zyflo

  • Indications
  1. Severe Persistent Asthma
    1. Adjunct only
    2. Other Leukotriene Modifiers are preferred
  • Dosing
  1. Approved only in age >=12 years and only as adjunct in Severe Asthma
  2. Dose: 1200 mg orally two times daily
  • Mechanism
  1. Attenuates bronchoconstriction and inflammation
  2. Leukotriene Synthesis Inhibitor (inhibits 5-lipoxygenase)
    1. Contrast with Leukotriene Receptor Antagonists (Zafirlukast or Accolate, Montelukast or Singulair)
  • Adverse Effects
  1. See Leukotriene Receptor Antagonist
  2. More adverse effects than other Leukotriene Modifiers (e.g. Montelukast, Zafirlukast)
  3. Dyspepsia
  4. Nausea
  5. Hepatotoxicity (5% of patients)
    1. Monitor liver enzymes every 3 months
  • Safety
  1. Pregnancy Category C
  2. Unknown safety in Lactation
  • Drug Interactions
  1. Zileuton increases other drug levels, potentiating their action
    1. Warfarin
    2. Theophylline
    3. Propranolol