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

Ontology: zileuton (C0081408)

Definition (NCI_NCI-GLOSS) A substance that is used to prevent asthma symptoms and that is being studied in the prevention of lung cancer. It belongs to the family of drugs called leukotriene blockers.
Definition (NCI) A synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma. (NCI04)
Definition (PDQ) A synthetic derivative of hydroxyurea with antiasthmatic properties. The leukotriene inhibitor zileuton blocks 5-lipoxygenase, which catalyzes the formation of leukotrienes from arachidonic acid; causes bronchodilation; decreases bronchial mucous secretion and edema; and may prevent or decrease the symptoms of asthma. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=285649&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=285649&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C26667" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C063449
SnomedCT 386180009, 108617005
English N-(1-benzo(b)thien-2-ylethyl)-N-hydroxyurea, zileuton, (+-)-N-Hydroxy-N-(1-benzo[b]thien-2-ylethyl)-urea, N-(1-Benzo[b]thien-2-ylethyl)-N-hydroxyurea, zileuton (Zyflo), zileuton (medication), ZILEUTON, zileuton [Chemical/Ingredient], Zileuton (product), Zileuton (substance), Zileuton, ZLT
Spanish zileutona, zileutón, zileutón (producto), zileutona (sustancia), zileutona (producto), zileutón (sustancia)

Ontology: Zyflo (C0724508)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C063449
English Zyflo, zyflo, Abbott brand of zileuton