II. Indications: Adjunctive in Asthma and Allergic Rhinitis

III. Dosing

  1. Avoid at mealtime
    1. Take 1 hour before or 2 hours after meals
  2. Dose
    1. Age >=12 years old: 20 mg orally twice daily
    2. Child 5-11 years old: 10 mg orally twice daily

IV. Mechanism

  1. Attenuates bronchoconstriction and inflammation
  2. Leukotriene Receptor Antagonist (competitive inhibitor at D4 and E4 receptors)
    1. Similar to Montelukast (Singulair)
    2. Contrast with Leukotriene Synthesis Inhibitor (Zileuton or Zyflo)

V. Adverse Effects

  1. See Leukotriene Receptor Antagonist
  2. Nausea
  3. Hepatotoxicity risk

VI. Efficacy

VII. Safety

  1. Pregnancy Category B
  2. Avoid in Lactation

VIII. Drug Interactions

  1. Zafirlukast increases other drug levels, potentiating their action
    1. Warfarin
    2. Theophylline
  2. Other drugs decrease Zafirlukast levels
    1. Erythromycin
    2. Theophylline
  3. Other drugs increase Zafirlukast levels
    1. Aspirin (high dose)

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Related Studies

Cost: Medications

zafirlukast (on 11/23/2022 at Medicaid.Gov Survey of pharmacy drug pricing)
ZAFIRLUKAST 10 MG TABLET Generic $0.87 each
ZAFIRLUKAST 20 MG TABLET Generic $0.91 each

Ontology: zafirlukast (C0378466)

Definition (NCI_NCI-GLOSS) A drug used to prevent and treat symptoms of asthma. It blocks substances that cause inflammation in the lungs. It is a type of antiasthmatic agent and a leukotriene receptor antagonist.
Definition (NCI) A toyl compound with anti-asthmatic property. Zafirlukast selectively and competitively binds and blocks the cysteinyl leukotriene 1 receptor , thereby preventing potent proinflammatory mediators leukotriene C4, D4 and E4 from binding. This prevents leukotriene-mediated actions, including enhanced migration of eosinophils and neutrophils, increased adhesion of leukocytes, increased monocyte and neutrophil aggregation, increased airway edema, inflammation, capillary permeability and bronchoconstriction.
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C062735
SnomedCT 320888004, 108614003, 386880006
English 4-(5-cyclopentyloxycarbonylamino-2-methylindol-3-yl-methyl)-3-methoxy-N-O-tolylsulfonylbenzamide, zafirlukast, Carbamic Acid,(3-((2-methoxy-4-((((2-methylphenyl)sulfonyl)amino)carbonyl)phenyl)methyl)-1-methyl-1H-indol-5-yl)-, Cyclopentyl Ester, Cyclopentyl 3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-methylindole-5-carbamate, zafirlukast (medication), zafirlukast [Chemical/Ingredient], ZAFIRLUKAST, Zafirlukast, Zafirlukast (product), Zafirlukast (substance)
Spanish zafirlukast (producto), zafirlukast (sustancia), zafirlukast

Ontology: Accolate (C0526502)

Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH C062735
English Accolate, accolate, AstraZeneca brand of zafirlukast, Zeneca brand of zafirkulast