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Zafirlukast

Leukotriene Receptor Antagonist · Antiasthmatic

Leukotriene Receptor AntagonistAntiasthmatic
CDSCO approvedSchedule H
EXCRETION
not curated
INTERACTIONS
11 major
SEVERE in our sources
PREGNANCY
not curated
Top interactionssee all 12
  • FentanylSevereDatabaseDDInter
  • HalofantrineSevereDatabaseDDInter
  • LeflunomideSevereDatabaseDDInter
  • LemborexantSevereDatabaseDDInter

Mechanism

Zafirlukast is a selective cysteinyl leukotriene (CysLT) receptor antagonist. It prevents the activation of the CysLT1 receptor, thereby blocking the inflammatory effects mediated by leukotrienes. This action contributes to its efficacy in treating asthma. Additionally, zafirlukast is known to inhibit hepatic enzyme CYP2C9.

Indications

Mild to moderate asthmaBronchial asthmaProphylactic therapy of mild-to-moderate asthma (as alternatives to inhaled glucocorticoids)Aspirin-induced asthmaExercise-induced asthma

Dosing

Adult
Resistance to Warfarin. Some patients require >20 mg/day of warfarin to achieve a therapeutic INR. These patients often have excessive vitamin K intake from the diet or parenteral supplementation.. VKORC1 gene have been identified in some of these patients (Rost. <1.5 mg/day of warfarin to achieve an INR of 2-3.…
Pediatric
5–11 yr 10 mg BD

Pharmacokinetics

Half-life
8–12 hours
Bioavailability
Well absorbed orally
Protein binding
Highly plasma protein bound
Metabolism
Metabolized by CYP2C9

Contraindications

  • Not to be used for terminating asthma episodes
  • No value in COPD

Side effects

Common
HeadacheRashes
Serious
  • Eosinophilia (infrequent)
  • Neuropathy (infrequent)
  • Churg-Strauss syndrome (few cases reported)

Drug interactions

Fentanyl
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Halofantrine
Severe
Database

Clinical effect not specified

Source: DDInter

Leflunomide
Severe
Database

Clinical effect not specified

Source: DDInter

Lemborexant
Severe
Database

Clinical effect not specified

Source: DDInter

Levacetylmethadol
Severe
Database

Clinical effect not specified

Source: DDInter

Lomitapide
Severe
Database

Clinical effect not specified

Source: DDInter

Lonafarnib
Severe
Database

Clinical effect not specified

Source: DDInter

Mipomersen
Severe
Database

Clinical effect not specified

Source: DDInter

Pexidartinib
Severe
Database

Clinical effect not specified

Source: DDInter

Pimozide
Severe
Database

Clinical effect not specified

Source: DDInter

Teriflunomide
Severe
Database

Clinical effect not specified

Source: DDInter

Theophylline
Moderate
Database

Zafirlukast decreases the clearance of theophylline, which can increase its plasma concentration and risk of toxicity.

Monitor theophylline plasma concentrations and adjust theophylline dose as needed to avoid toxicity.

Source: DDInter

Related guidelines

Other Leukotriene Receptor Antagonist drugs

Ask House about Zafirlukast

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Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e·Verified: 2026-05-13 · House clinical team