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Zileuton
Overview
What is Zileuton?
Zileuton is an orally active inhibitor of 5‑lipoxygenase, the enzyme that catalyzes the formation of leukotrienes from arachidonic acid. Zileuton has the chemical name (±)-1-(1-Benzo[b]thien-2-ylethyl)-1-hydroxyurea and the following chemical structure:
Zileuton has the molecular formula CHNOS and a molecular weight of 236.29. It is a racemic mixture (50:50) of R(+) and S(-) enantiomers. Zileuton is a practically odorless, white, crystalline powder that is soluble in methanol and ethanol, slightly soluble in acetonitrile, and practically insoluble in water and hexane. The melting point ranges from 144.2ºC to 145.2ºC.
Zileuton Extended-Release Tablets for oral administration are triple-layer tablets comprised of an immediate-release layer, a middle (barrier) layer, and an extended-release layer. Zileuton Extended-Release Tablets are oblong, film-coated tablets with one red layer between two white layers, debossed on one side with “CT2”. Each tablet contains 600 mg of zileuton and the following inactive ingredients: crospovidone, ferric oxide, glyceryl behenate, hydroxypropyl cellulose, hypromellose, magnesium stearate, mannitol, microcrystalline cellulose, povidone, pregelatinized starch, propylene glycol, sodium starch glycolate, and talc.
What does Zileuton look like?
What are the available doses of Zileuton?
Extended-release tablets: 600 mg. ()
What should I talk to my health care provider before I take Zileuton?
Information on specific populations is based on studies conducted with zileuton immediate-release tablets and is applicable to Zileuton Extended-Release Tablets.
How should I use Zileuton?
Zileuton Extended-Release Tablets is indicated for the prophylaxis and chronic treatment of asthma in adults and children 12 years of age and older.
Zileuton Extended-Release Tablets is not indicated for use in the reversal of bronchospasm in acute asthma attacks. Therapy with Zileuton Extended-Release Tablets can be continued during acute exacerbations of asthma.
The recommended dosage of Zileuton Extended-Release Tablets for the treatment of patients with asthma is two 600 mg extended-release tablets twice daily, within one hour after morning and evening meals, for a total daily dose of 2400 mg. Tablets should not be chewed, cut or crushed. If a dose is missed, the patient should take the next dose at the scheduled time and not double the dose. Assess hepatic function enzymes prior to initiation of Zileuton Extended-Release Tablets and periodically during treatment [seeand].
What interacts with Zileuton?
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What are the warnings of Zileuton?
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What are the precautions of Zileuton?
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What are the side effects of Zileuton?
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What should I look out for while using Zileuton?
The use of Zileuton Extended-Release Tablets is contraindicated in patients with:
What might happen if I take too much Zileuton?
Human experience of acute overdose with zileuton is limited. A patient in a clinical study took between 6.6 and 9.0 grams of zileuton immediate-release tablets in a single dose. Vomiting was induced and the patient recovered without sequelae. Zileuton is not removed by dialysis. Should an overdose occur, the patient should be treated symptomatically and supportive measures instituted as required. If indicated, elimination of unabsorbed drug should be achieved by emesis or gastric lavage; usual precautions should be observed to maintain the airway. A Certified Poison Control Center should be consulted for up-to-date information on management of overdose with Zileuton Extended-Release Tablets.
The oral minimum lethal doses in mice and rats were 500-4000 and 300-1000 mg/kg, respectively (providing greater than 3 and 9 times the systemic exposure [AUC] achieved at the maximum recommended human daily oral dose, respectively). In dogs, at an oral dose of 1000 mg/kg (providing in excess of 12 times the systemic exposure [AUC] achieved at the maximum recommended human daily oral dose) no deaths occurred but nephritis was reported.
How should I store and handle Zileuton?
Store between 20°C and 25°C (68°F and 77°F) Excursions permitted between 15°C and 30°C (59°F and 86°F).Protect from light.Store between 20°C and 25°C (68°F and 77°F) Excursions permitted between 15°C and 30°C (59°F and 86°F).Protect from light.Zileuton Extended-Release Tablets are debossed on one side with “CT2”; they are available in bottles of 120 tablets (NDC 66993-485-32).Store at 20°C to 25°C (68°F to 77ºF); excursions permitted between 15°C and 30°C (between 59°F and 86ºF). [see USP Controlled Room Temperature]. Protect from light.Zileuton Extended-Release Tablets are debossed on one side with “CT2”; they are available in bottles of 120 tablets (NDC 66993-485-32).Store at 20°C to 25°C (68°F to 77ºF); excursions permitted between 15°C and 30°C (between 59°F and 86ºF). [see USP Controlled Room Temperature]. Protect from light.
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Zileuton is an inhibitor of 5-lipoxygenase and thus inhibits leukotriene (LTB, LTC, LTD and LTE) formation. Both the R(+) and S(-) enantiomers are pharmacologically active as 5-lipoxygenase inhibitors in and systems. 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. LTB, a chemoattractant for neutrophils and eosinophils, and cysteinyl leukotrienes (LTC, LTD, LTE) can be measured in a number of biological fluids including bronchoalveolar lavage fluid (BALF), blood, urine and sputum from asthmatic patients.
Zileuton is an orally active inhibitor of LTB formation in several species, including mice, rats, rabbits, dogs, sheep, and monkeys. Zileuton inhibits arachidonic acid-induced ear edema in mice, neutrophil migration in mice in response to polyacrylamide gel, and eosinophil migration into the lungs of antigen-challenged sheep. In a mouse model of allergic inflammation, zileuton inhibited neutrophil and eosinophil influx, reduced the levels of multiple cytokines in the BALF, and reduced serum IgE levels. Zileuton inhibits leukotriene-dependent smooth muscle contractions in guinea pig and human airways. The compound inhibits leukotriene-dependent bronchospasm in antigen and arachidonic acid-challenged guinea pigs. In antigen-challenged sheep, zileuton inhibits late-phase bronchoconstriction and airway hyperreactivity. The clinical relevance of these findings is unknown.
Non-Clinical Toxicology
The use of Zileuton Extended-Release Tablets is contraindicated in patients with:Cyclobenzaprine HCl may have life-threatening interactions with MAO inhibitors. (See .) Postmarketing cases of serotonin syndrome have been reported during combined use of Cyclobenzaprine Hydrochloride and other drugs, such as SSRIs, SNRIs, TCAs, tramadol, bupropion, meperidine, verapamil, or MAO inhibitors. If concomitant treatment with Cyclobenzaprine Hydrochloride and other serotonergic drugs is clinically warranted, careful observation is advised, particularly during treatment initiation or dose increases (see ).
Cyclobenzaprine HCl may enhance the effects of alcohol, barbiturates, and other CNS depressants.
Tricyclic antidepressants may block the antihypertensive action of guanethidine and similarly acting compounds.
Tricyclic antidepressants may enhance the seizure risk in patients taking tramadol.
† ULTRAM (tramadol hydrochloride tablets, Ortho-McNeil Pharmaceutical)
† ULTRACET (tramadol hydrochloride and acetaminophen tablets, Ortho-McNeil Pharmaceutical)
Elevations of one or more hepatic function enzymes and bilirubin may occur during Zileuton Extended-Release Tablets therapy. These laboratory abnormalities may progress to clinically significant liver injury, remain unchanged, or resolve with continued treatment, usually within three weeks. The ALT (SGPT) test is considered the most sensitive indicator of liver injury for Zileuton Extended-Release Tablets.
Assess hepatic function enzymes prior to initiation of, and during therapy with, Zileuton Extended-Release Tablets. Assess serum ALT before treatment begins, once a month for the first 3 months, every 2-3 months for the remainder of the first year, and periodically thereafter for patients receiving long-term Zileuton Extended-Release Tablets therapy. If clinical signs and/or symptoms of liver dysfunction develop (e.g., right upper quadrant pain, nausea, fatigue, lethargy, pruritus, jaundice, or “flu-like” symptoms) or transaminase elevations ≥5xULN occur, discontinue Zileuton Extended-Release Tablets and follow hepatic function enzymes until normal.
In controlled and open-label clinical studies involving more than 5000 patients treated with zileuton immediate-release tablets, the overall rate of ALT elevation ≥3xULN was 3.2%. In these trials, one patient developed symptomatic hepatitis with jaundice, which resolved upon discontinuation of therapy. An additional 3 patients with transaminase elevations developed mild hyperbilirubinemia that was less than 3xULN. There was no evidence of hypersensitivity or other alternative etiologies for these findings.
Since treatment with Zileuton Extended-Release Tablets may result in increased hepatic function enzymes and liver injury, Zileuton Extended-Release Tablets should be used with caution in patients who consume substantial quantities of alcohol and/or have a past history of liver disease.
Hepatotoxicity:Elevations of one or more hepatic function enzymes and bilirubin may occur during Zileuton Extended-Release Tablets therapy [see].
The most commonly occurring adverse reactions (≥5%) with Zileuton Extended-Release Tablets are sinusitis, nausea, and pharyngolaryngeal pain.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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