Zileuton
- Atc Codes:R03DX
- CAS Codes:111406-87-2
- PHARMGKB ID:111406-87-2
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
North America
USA: Zyflo.
Drug combinations
Chemistry
Zileuton: C~11~H~12~N~2~O~2~S. Mw: 236.29. (1) Urea, N-(1-benzo[b]thien-2-ylethyl)-N-hydroxy-, (±)-; (2)(±)-1-(1-Benzo[b]thien-2-ylethyl)-1-hydroxyurea. CAS-111406-87-2 (1990).
Pharmacologic Category
Anti-inflammatory Agents; Leukotriene Modifiers; 5-Lipoxygenase Inhibitor. (ATC-Code: R03DX).
Mechanism of action
Specific 5-lipoxygenase inhibitor (ALOX5) which inhibits leukotriene formation. Leukotrienes augment neutrophil and eosinophil migration, neutrophil and monocyte aggregation, leukocyte adhesion, increased capillary permeability, and smooth muscle contraction (which contribute to inflammation, edema, mucous secretion, and bronchoconstriction in airway of the asthmatic.)
Therapeutic use
Prophylaxis and chronic treatment of asthma in children ≥12 years of age and adults.
Pregnancy and lactiation implications
Reduced body weight and increased skeletal variations observed in rats. There are no adequate, well-controlled studies in pregnant women. Excretion in breast milk unknown (not recommended during lactation).
Unlabeled use
Contraindications
Hypersensitivity to zileuton or any component of the formulation. Active liver disease or transaminase elevations greater than or equal to 3 times upper limit of normal (≥3 times ULN).
Warnings and precautions
Reports exist of hepatotoxicity (elevated transaminase levels). Females >65 years and patients with pre-existing elevated transaminases may be at greater risk. Use caution with history of liver disease and/or in patients who consume substantial quantities of ethanol. Not FDA approved for reversal of bronchospasm in acute asthma attacks, including status asthmaticus.