Leflunomide
Severe
Database
Clinical effect not specified
Source: DDInter
Drug reference
Zileuton
Leukotriene Receptor Antagonist · Anti-asthmatic
Leukotriene Receptor AntagonistAnti-asthmatic
CDSCO approvedSchedule H
EXCRETION
—
not curated
INTERACTIONS
9 major
SEVERE in our sources
PREGNANCY
—
not curated
Top interactionssee all 12 →
- LeflunomideSevereDatabaseDDInter
- LomitapideSevereDatabaseDDInter
- MipomersenSevereDatabaseDDInter
- PexidartinibSevereDatabaseDDInter
Mechanism
Zileuton is a 5-lipoxygenase (5-LOX) inhibitor. It prevents the oxygenation of arachidonic acid (AA) at C5, blocking the formation of 5-HPETE and LTA4. This action ultimately reduces the synthesis of various leukotrienes, including LTB4 and the cysteinyl leukotrienes (LTC4, LTD4, LTE4), which are key mediators of inflammation.
Indications
Mild to moderate asthmaAsthma (used briefly, then withdrawn)Asthma (clinical efficacy similar to montelukast)
Dosing
- Adult
- 1-2 mg/kg/day of prednisone for 5 days. Oral corticosteroids. sulfate is 25-75 mg/kg (maximum 2.0 g) intravenously
Pharmacokinetics
Duration
Short duration of action
Side effects
Common
increased liver function tests (transaminases)
Serious
- Hepatotoxic potential
Drug interactions
Lomitapide
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
Rasagiline
Severe
Database
Clinical effect not specified
Source: DDInter
Terfenadine
Severe
Database
Clinical effect not specified
Source: DDInter
Teriflunomide
Severe
Database
Clinical effect not specified
Source: DDInter
Tizanidine
Severe
Database
Clinical effect not specified
Source: DDInter
Chlorpromazine
Moderate
Textbook
Increased chlorpromazine exposure (up to 38%).
Monitor for increased side effects; dose reduction may be needed.
Source: G&G 14e · p369
Haloperidol
Moderate
Textbook
Increased haloperidol exposure (average 62.5%).
Monitor for increased side effects; dose reduction may be needed.
Source: G&G 14e · p369
Theophylline
Moderate
Database
Zileuton 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 Zileuton
Continue into a citation-backed clinical answer with the drug context already attached.
Sources: KD Tripathi 7e, Goodman & Gilman 14e, Harrison 22e, Nelson·Verified: 2026-05-10 · House clinical team