API

ZILEUTON

Drug classification

Dosage form

TABLET;ORAL

API strength per dosage

600MG

Dose

Adults and adolescents ≥12 years: 600 mg orally four times daily. Not recommended for pediatric patients under 12 years. Use with caution in hepatic impairment; contraindicated in active liver disease or persistent ALT/AST elevations ≥3× ULN. Regular liver function monitoring is required.

Mechanism of action

Inhibits 5-lipoxygenase (ALOX5), the enzyme catalyzing leukotriene synthesis from arachidonic acid, thereby reducing formation of leukotriene B4, C4, D4, and E4, which mediate bronchoconstriction, inflammation, and edema in asthma.

Indications

Prophylaxis and chronic treatment of asthma in adults and children 12 years of age and older.

Side effects

Pregnancy category

Category C

Precautions

Liver dysfunction, monitor liver enzymes, contraindicated in active liver disease, use caution with alcohol, potential drug interactions (theophylline, warfarin, propranolol), not recommended in children under 12, risk of neuropsychiatric events, discontinue if signs of liver injury occur, use in pregnancy only if clearly needed.

Contraindications

Active liver disease, persistent alanine aminotransferase (ALT) elevations ≥3 times the upper limit of normal, hypersensitivity to zileuton or any component of the formulation.