II. Indications

  1. Severe Persistent Asthma
    1. Adjunct only
    2. Other Leukotriene Modifiers are preferred

III. Dosing

  1. Approved only in age >=12 years and only as adjunct in Severe Asthma
  2. Dose: 1200 mg orally two times daily

IV. 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)

V. 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

VI. Efficacy

VII. Safety

  1. Pregnancy Category C
  2. Unknown safety in Lactation

VIII. Drug Interactions

  1. Zileuton increases other drug levels, potentiating their action
    1. Warfarin
    2. Theophylline
    3. Propranolol

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Related Studies

Cost: Medications

zileuton (on 6/7/2023 at Medicaid.Gov Survey of pharmacy drug pricing)
ZILEUTON ER 600 MG TABLET Generic $10.02 each