Zafirlukast

Aka: Zafirlukast, Accolate

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II. Indications: Adjunctive in Asthma and Allergic Rhinitis

  1. Moderate Persistent Asthma
  2. Severe Persistent Asthma
  3. Aspirin-induced Asthma
  4. Exercise-Induced Bronchospasm
  5. 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

  1. See See Leukotriene Receptor Antagonist

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)

IX. Resources

  1. Zafirlukast (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=0262e192-94f4-423d-a58e-bb374dc106fe

X. References

  1. (2020) Drugs for Asthma, Med Lett Drug Ther 62: 193-200
  2. (1996) Med Lett Drugs Ther 38:111-2 [PubMed]
  3. (2000) Med Lett Drugs Ther 42:22-3 [PubMed]
  4. Scow (2007) Am Fam Physician 75:65-70 [PubMed]
  5. Wilson (2001) Chest 119:2021-6 [PubMed]

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