II. Indications: Adjunctive in Asthma and Allergic Rhinitis
III. Dosing
- Avoid at mealtime
- Take 1 hour before or 2 hours after meals
- Dose
- Age >=12 years old: 20 mg orally twice daily
- Child 5-11 years old: 10 mg orally twice daily
IV. Mechanism
- Attenuates bronchoconstriction and inflammation
-
Leukotriene Receptor Antagonist (competitive inhibitor at D4 and E4 receptors)
- Similar to Montelukast (Singulair)
- Contrast with Leukotriene Synthesis Inhibitor (Zileuton or Zyflo)
V. Adverse Effects
- See Leukotriene Receptor Antagonist
- Nausea
- Hepatotoxicity risk
VI. Efficacy
- See See Leukotriene Receptor Antagonist
VII. Safety
- Pregnancy Category B
- Avoid in Lactation
VIII. Drug Interactions
- Zafirlukast increases other drug levels, potentiating their action
- Other drugs decrease Zafirlukast levels
- Other drugs increase Zafirlukast levels
- Aspirin (high dose)
IX. Resources
X. References
- (2020) Drugs for Asthma, Med Lett Drug Ther 62: 193-200
- (1996) Med Lett Drugs Ther 38:111-2 [PubMed]
- (2000) Med Lett Drugs Ther 42:22-3 [PubMed]
- Scow (2007) Am Fam Physician 75:65-70 [PubMed]
- Wilson (2001) Chest 119:2021-6 [PubMed]
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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 |