Zileuton
Zileuton Uses, Dosage, Side Effects, Food Interaction and all others data.
Leukotrienes are substances that induce numerous biological effects including augmentation of neutrophil and eosinophil migration, neutrophil and monocyte aggregation, leukocyte adhesion, increased capillary permeability, and smooth muscle contraction. These effects contribute to inflammation, edema, mucus secretion, and bronchoconstriction in the airways of asthmatic patients. Zileuton relieves such symptoms through its selective inhibition of 5-lipoxygenase, the enzyme that catalyzes the formation of leukotrienes from arachidonic acid. Specifically, it inhibits leukotriene LTB4, LTC4, LTD4, and LTE4 formation. Both the R(+) and S(-) enantiomers are pharmacologically active as 5-lipoxygenase inhibitors in in vitro systems. The immediate release tablet of Zileuton has been withdrawn from the US market.
Zileuton is an asthma drug that differs chemically and pharmacologically from other antiasthmatic agents. It blocks leukotriene synthesis by inhibiting 5-lipoxygenase, an enzyme of the eicosanoid synthesis pathway. Current data indicates that asthma is a chronic inflammatory disorder of the airways involving the production and activity of several endogenous inflammatory mediators, including leukotrienes. Sulfido-peptide leukotrienes (LTC4, LTD4, LTE4, also known as the slow-releasing substances of anaphylaxis) and LTB4, a chemoattractant for neutrophils and eosinophils, are derived from the initial unstable product of arachidonic acid metabolism, leukotriene A4 (LTA4), and can be measured in a number of biological fluids including bronchoalveolar lavage fluid (BALF) from asthmatic patients. In humans, pretreatment with zileuton attenuated bronchoconstriction caused by cold air challenge in patients with asthma.
| Trade Name | Zileuton |
| Availability | Prescription only |
| Generic | Zileuton |
| Zileuton Other Names | Leutrol, Zileuton, Zileutón, Zileutonum |
| Related Drugs | Dupixent, Xolair, ProAir Digihaler, Symbicort, Breo Ellipta, Ventolin, Xopenex, Ventolin HFA |
| Weight | 600mg, 600mg |
| Type | Oral tablet, oral tablet, extended release |
| Formula | C11H12N2O2S |
| Weight | Average: 236.29 Monoisotopic: 236.061948328 |
| Protein binding | 93% bound to plasma proteins, primarily to albumin. |
| Groups | Approved, Investigational, Withdrawn |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Zileuton is a leukotriene synthesis inhibitor used in the prophylaxis and treatment of chronic asthma.
For the prophylaxis and chronic treatment of asthma in adults and children 12 years of age and older.
Zileuton is also used to associated treatment for these conditions: Asthma, Chronic Asthma
How Zileuton works
Leukotrienes are substances that induce numerous biological effects including augmentation of neutrophil and eosinophil migration, neutrophil and monocyte aggregation, leukocyte adhesion, increased capillary permeability, and smooth muscle contraction. These effects contribute to inflammation, edema, mucus secretion, and bronchoconstriction in the airways of asthmatic patients. Zileuton relieves such symptoms through its selective inhibition of 5-lipoxygenase, the enzyme that catalyzes the formation of leukotrienes from arachidonic acid. Specifically, it inhibits leukotriene LTB4, LTC4, LTD4, and LTE4 formation. Both the R(+) and S(-) enantiomers are pharmacologically active as 5-lipoxygenase inhibitors in in vitro systems. Due to the role of leukotrienes in the pathogenesis of asthma, modulation of leukotriene formation by interruption of 5-lipoxygenase activity may reduce airway symptoms, decrease bronchial smooth muscle tone, and improve asthma control.
Toxicity
Minimum oral lethal dose of zileuton in various preparations was 500-4000 mg/kg in mice and 300-1000 mg/kg in rats (providing greater than 3 and 9 times the systemic exposure [AUC] achieved at the maximum recommended human daily oral dose, respectively).
Food Interaction
- Take with food. The AUC and Cmin of zileuton extended-release tablets are increased by food, and therefore should be taken with meals.
- Take with or without food. ZYFLO (zileuton) regular release tablets can be taken with or without food.
Zileuton Drug Interaction
Unknown: fluticasone / salmeterol, fexofenadine, aspirin, amoxicillin / clavulanate, sulfamethoxazole / trimethoprim, diphenhydramine, calcium / vitamin d, escitalopram, atorvastatin, guaifenesin, albuterol, tiotropium, budesonide / formoterol, dulaglutide, acetaminophen, albuterol, cyanocobalamin, ascorbic acid, cholecalciferol, ondansetron
Zileuton Disease Interaction
Volume of Distribution
- 1.2 L/kg
Elimination Route
Rapidly and almost completely absorbed. The absolute bioavailability is unknown.
Half Life
2.5 hours
Clearance
- Apparent oral cl=7 mL/min/kg
Elimination Route
Elimination of zileuton is predominantly via metabolism with a mean terminal half-life of 2.5 hours. The urinary excretion of the inactive N-dehydroxylated metabolite and unchanged zileuton each accounted for less than 0.5% of the dose.
Innovators Monograph
You find simplified version here Zileuton
