Zafirlukast
ACCOLATE
Pronunciation: za-FIR-loo-kast
What it isCysteinyl-leukotriene receptor antagonist; maintenance treatment of asthma.
Why this oneUnlike montelukast, it has clinically important warfarin and food interactions and greater hepatotoxicity concern.
What limits itTake on an empty stomach and monitor liver symptoms; CYP2C9 inhibition can raise warfarin and requires closer INR monitoring.
FDA-approved for
- asthma maintenance (1996)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Asthma (prophylaxis and chronic treatment) | adults & children ≥12 yr | 20 mg BID | 20 mg BID | 20 mg BID |
| Asthma | children 5-11 yr | 10 mg BID | 10 mg BID | 10 mg BID |
Renal No adjustment needed
Hepatic Contraindicated (hepatic impairment including cirrhosis)
Instructions
- Take ≥1 hour before or 2 hours after meals (food reduces bioavailability)
Available strengths
- tab 10, 20 mg
Contraindications
- Hepatic impairment, including hepatic cirrhosis
Cautions
- Hepatotoxicity (symptomatic hepatitis, rare hepatic failure) — predominantly in females
- Eosinophilic conditions / Churg-Strauss syndrome
- Neuropsychiatric events (insomnia, depression)
- Hypersensitivity reactions (urticaria, angioedema)
Adverse reactions
- Headache
- Nausea
- Diarrhea
- Abdominal pain
- Elevated ALT (SGPT)
Pregnancy Undefined
Lactation Undefined
Cost
Generic entry2010
NO BOXED WARNINGS
Principal riskIt inhibits CYP2C9 and raises warfarin
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityTremor, tachycardia or anticholinergic effects; excessive beta-agonist exposure can cause hypokalemia and arrhythmia.