Dosing & Uses
Dosage Forms & Strengths
tablet
- 600mg
tablet, extended release
- 600mg
Asthma
Extended release: 1200 mg PO twice daily, within 1 hour after morning and evening meals
Conventional: 600 mg PO four times daily
Monitor: LFTs
Contraindicated in hepatic dysfunction
Dosage Forms & Strengths
tablet
- 600mg
tablet, extended release
- 600mg
Asthma
<12 years
- Safety and efficacy not established
- The FDA has not required pediatric studies in patients <12 years old due to the risk of hepatotoxicity; not recommeded for children younger than 12 years
>12 years
- Extended Release: 1200 mg PO twice daily, within 1 hour after morning and evening meals
- Conventional: 600 mg PO four times daily
- Monitor: LFTs
- Contraindicated in hepatic dysfunction
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
Contraindicated (1)
- flibanserin
zileuton will increase the level or effect of flibanserin by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Contraindicated. Coadministration of flibanserin with moderate or strong CYP3A4 inhibitors is contraindicated. Severe hypotension or syncope can occur.
Serious - Use Alternative (16)
- alosetron
zileuton will increase the level or effect of alosetron by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- cobimetinib
zileuton will increase the level or effect of cobimetinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If concurrent short term (14 days or less) use of moderate CYP3A inhibitors is unavoidable for patients who are taking cobimetinib 60 mg, reduce the cobimetinib dose to 20 mg. After discontinuation of a moderate CYP3A inhibitor, resume cobimetinib 60 mg. Use an alternative to a moderate CYP3A inhibitor in patients who are taking a reduced dose of cobimetinib (40 or 20 mg daily).
- duloxetine
zileuton will increase the level or effect of duloxetine by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
- eliglustat
zileuton increases levels of eliglustat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Moderate CYP3A4 inhibitors are not recommended with eliglustat poor or intermediate metabolizers; reduce eliglustat dose from 84 mg BID to 84 mg once daily in extensive metabolizers .
- fentanyl
zileuton will increase the level or effect of fentanyl by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of CYP3A4 inhibitors with fentanyl is necessary, monitor patients for respiratory depression and sedation at frequent intervals and consider fentanyl dose adjustments until stable drug effects are achieved.
- fentanyl intranasal
zileuton will increase the level or effect of fentanyl intranasal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of CYP3A4 inhibitors with fentanyl is necessary, monitor patients for respiratory depression and sedation at frequent intervals and consider fentanyl dose adjustments until stable drug effects are achieved.
- fentanyl transdermal
zileuton will increase the level or effect of fentanyl transdermal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of CYP3A4 inhibitors with fentanyl is necessary, monitor patients for respiratory depression and sedation at frequent intervals and consider fentanyl dose adjustments until stable drug effects are achieved.
- fentanyl transmucosal
zileuton will increase the level or effect of fentanyl transmucosal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of CYP3A4 inhibitors with fentanyl is necessary, monitor patients for respiratory depression and sedation at frequent intervals and consider fentanyl dose adjustments until stable drug effects are achieved.
- irinotecan liposomal
zileuton will increase the level or effect of irinotecan liposomal by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.
- ivabradine
zileuton will increase the level or effect of ivabradine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid coadministration of ivabradine with moderate CYP3A4 inhibitors.
- lonafarnib
zileuton will increase the level or effect of lonafarnib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration of lonafarnib (a sensitive CYP3A substrate) with weak CYP3A inhibitors is unavoidable, reduce to, or continue lonafarnib at starting dose. Closely monitor for arrhythmias and events (eg, syncope, heart palpitations) since lonafarnib effect on QT interval is unknown.
- naloxegol
zileuton will increase the level or effect of naloxegol by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministation of naloxegol with moderate CYP3A4 inhibitors is unavoidable, reduce naloxegol dose to 12.5 mg qDay
- olaparib
zileuton will increase the level or effect of olaparib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. If coadministration with moderate CYP3A inhibitors cannot be avoided, reduce olaparib dose to 200 mg (capsule) or 150 mg (tablet) PO BID. Do not substitute tablets with capsules.
- pimozide
zileuton increases levels of pimozide by decreasing metabolism. Contraindicated. May prolong QTc interval.
- pirfenidone
zileuton will increase the level or effect of pirfenidone by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug. Use of strong CYP1A2 inhibitors should be discontinued before initiating pirfenidone and avoided during treatment; if strong CYP1A2 inhibitors are the only drug of choice, dosage reductions are recommended
- tizanidine
zileuton will increase the level or effect of tizanidine by affecting hepatic enzyme CYP1A2 metabolism. Avoid or Use Alternate Drug.
Monitor Closely (40)
- atazanavir
atazanavir increases levels of zileuton by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Potential for increased toxicity. .
- atogepant
zileuton will increase the level or effect of atogepant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- avapritinib
zileuton will increase the level or effect of avapritinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- bendamustine
zileuton increases levels of bendamustine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Decreased conversion of bendamustine to active metabolites. Concentration of active metabolites of bendamustine may be decreased.
- brexpiprazole
zileuton will increase the level or effect of brexpiprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Administer a quarter of brexpiprazole dose if coadministered with a moderate CYP3A4 inhibitor PLUS a strong/moderate CYP2D6 inhibitor.
- clomipramine
zileuton will increase the level or effect of clomipramine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- clozapine
zileuton will increase the level or effect of clozapine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- darunavir
darunavir increases levels of zileuton by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Potential for increased toxicity. .
- deferasirox
deferasirox will increase the level or effect of zileuton by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- difelikefalin
difelikefalin and zileuton both increase sedation. Use Caution/Monitor.
- eltrombopag
zileuton will increase the level or effect of eltrombopag by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- eluxadoline
zileuton increases levels of eluxadoline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. As a precautionary measure due to incomplete information on the metabolism of eluxadoline, use caution when coadministered with strong CYP1A2 inhibitors.
- finerenone
zileuton will increase the level or effect of finerenone by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Monitor serum potassium during initiation and dosage adjustment of either finererone or weak CYP3A4 inhibitors. Adjust finererone dosage as needed.
- fosamprenavir
fosamprenavir increases levels of zileuton by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Potential for increased toxicity. .
- imipramine
zileuton will increase the level or effect of imipramine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- indinavir
indinavir increases levels of zileuton by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Potential for increased toxicity. .
- isavuconazonium sulfate
zileuton will increase the level or effect of isavuconazonium sulfate by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lemborexant
zileuton will increase the level or effect of lemborexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Lower nightly dose of lemborexant recommended if coadministered with weak CYP3A4 inhibitors. See drug monograph for specific dosage modification.
- letermovir
letermovir increases levels of zileuton by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- lidocaine
zileuton will increase the level or effect of lidocaine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- lomitapide
zileuton increases levels of lomitapide by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lomitapide dose should not exceed 30 mg/day.
- lopinavir
lopinavir increases levels of zileuton by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Potential for increased toxicity.
- mefloquine
zileuton will increase the level or effect of mefloquine by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- mexiletine
zileuton will increase the level or effect of mexiletine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- nelfinavir
nelfinavir increases levels of zileuton by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Potential for increased toxicity. .
- olanzapine
zileuton will increase the level or effect of olanzapine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- palbociclib
zileuton will increase the level or effect of palbociclib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- pentoxifylline
zileuton will increase the level or effect of pentoxifylline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- ramelteon
zileuton will increase the level or effect of ramelteon by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- rasagiline
zileuton will increase the level or effect of rasagiline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Recommended dose of rasagiline is 0.5mg daily in combination with CYP1A2 inhibitors.
- ritonavir
ritonavir increases levels of zileuton by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Potential for increased toxicity. .
- ropinirole
zileuton will increase the level or effect of ropinirole by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- sonidegib
zileuton will increase the level or effect of sonidegib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Avoid coadministration of sonidegib with moderate CYP3A4 inhibitors. If a moderate CYP3A inhibitor must be used, administer the moderate CYP3A inhibitor for <14 days and monitor closely for adverse reactions, particularly musculoskeletal adverse reactions.
- suvorexant
zileuton will increase the level or effect of suvorexant by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Decrease suvorexant starting dose to 5 mg HS if coadministered with moderate CYP3A4 inhibitors
- tazemetostat
zileuton will increase the level or effect of tazemetostat by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- terbinafine
zileuton will increase the level or effect of terbinafine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- theophylline
zileuton will increase the level or effect of theophylline by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.
- tinidazole
zileuton will increase the level or effect of tinidazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.
- tofacitinib
zileuton increases levels of tofacitinib by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. No specific dose adjustment recommended when tofacitinib coadministered with moderate CYP3A4 inhibitors; decrease tofacitinib dose if coadministered with both moderate CYP3A4 and potent CYP2C19 inhibitors .
- warfarin
zileuton will increase the level or effect of warfarin by Other (see comment). Use Caution/Monitor. Warfarin's less potent R-enantiomer is metabolized in part by CYP3A4 (and also CYP1A2 and CYP2C19). Monitor INR more frequently if coadministered with inhibitors of these isoenzymes and adjust warfarin dose if needed.
Minor (6)
- antipyrine
zileuton will increase the level or effect of antipyrine by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.
- asenapine
zileuton will increase the level or effect of asenapine by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.
- caffeine
zileuton will increase the level or effect of caffeine by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.
- frovatriptan
zileuton will increase the level or effect of frovatriptan by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.
- ondansetron
zileuton will increase the level or effect of ondansetron by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown. No dosage adjustment is needed for ondansetron.
- riluzole
zileuton will increase the level or effect of riluzole by affecting hepatic enzyme CYP1A2 metabolism. Minor/Significance Unknown.
Adverse Effects
>10%
Headache (24.6%)
1-10%
Abdominal pain (5%)
ALT elevation ≥3 times ULN (1.9-5%)
Asthenia (3.8%)
Dyspepsia (8.2%)
Diarrhea (5%)
Generalized pain (7.8%)
Nausea (5.5%)
Leukopenia (1-3%)
Myalgia (7%)
Weakness (4%)
Sinusitis (7%)
Pharyngolaryngeal pain (5%)
< 1%
Hepatitis
Behavioral changes
Jaundice
Liver failure
Suicidality
Suicide
Warnings
Contraindications
Hypersensitivity
Liver disease, LFT's ≥3x ULN
Cautions
Not indicated for use in acute bronchospasm
History of liver disease, heavy alcohol use
Behavioral changes and sleep disorders reported
Not recommended for patients <12 years due to risk of hepatotoxicity
Pregnancy & Lactation
Pregnancy
There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to asthma medications during pregnancy; for more information, contact the MothersToBaby Pregnancy Studies conducted by Organization of Teratology Information Specialists at 1- 877-311-8972 or visit http://mothertobaby.org/pregnancy-studies
There are no adequate human data on use in pregnant women to inform a drug associated risk
Animal data
- In animal studies, oral administration to pregnant rats and rabbits during organogenesis produced adverse developmental outcomes; structural abnormalities (cleft palate) were observed in rabbits at a dose similar to maximum recommended human daily oral dose (MRHD), alterations to growth (reduced fetal body weight and increased skeletal variations) were observed in rats at maternal plasma exposures 20 times greater than at MRHD; in a pre- and post-natal development study, oral administration to pregnant rats from organogenesis through weaning at maternal plasma exposures 20 times greater than MRHD resulted in reduced pup survival and body weights; the drug and/or its metabolites cross placental barrier of rats; therefore, drug may be transmitted from mother to developing fetus
Lactation
The drug and metabolites are excreted in rat milk; it is not known if zileuton is excreted in human milk, nor are there data on effects of drug on breastfed infant or effects on maternal milk production; because many drugs are excreted in human milk, and because of potential for tumorigenicity shown in animal studies, the developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for drug and any potential adverse effects on breastfed child from drug or from the underlying maternal condition
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Inhibitor of 5-lipoxygenase, which inhibits formation of LTB4, LTC4, LTD4, & LTE4
Inhibition of leukotriene formation reduces eosinophil and neutrophil migration, neutrophil and monocyte aggregation, capillary permeability, and smooth muscle contraction
Pharmacokinetics
Half-Life: 2.5 hr
Onset: 2-5 hr
Peak Plasma Time: 1.7 hr
Protein Bound: 93%
Vd: 1.2 L/kg
Metabolites: O-glucuronide conjugate & N-dehydroxylated metabolite
Clearance: 7 mL/min/kg
Excretion: Urine (95%); feces (2%)
Enzymes inhibited: hepatic CYP1A2, CYP3A4, and CYP2C9
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| zileuton oral - | 600 mg tablet |  | |
| zileuton oral - | 600 mg tablet |  | |
| zileuton oral - | 600 mg tablet |  | |
| zileuton oral - | 600 mg tablet |  | |
| Zyflo oral - | 600 mg tablet |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
zileuton oral
ZILEUTON EXTENDED-RELEASE - ORAL
(zye-LOO-ton)
COMMON BRAND NAME(S): Zyflo CR
USES: Zileuton is used to control and prevent symptoms (such as wheezing and shortness of breath) caused by asthma. Controlling symptoms of asthma helps you maintain your normal activities and cuts down on time lost from work or school.This medication must be used regularly to be effective. It does not work right away and should not be used to relieve sudden asthma attacks. If an asthma attack occurs, use your quick-relief inhaler (such as albuterol, salbutamol) as prescribed.This drug is not recommended for use in children younger than 12 years due to possible risk of liver problems.
HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking zileuton and each time you get a refill. If you have any questions, ask your doctor or pharmacist.Take this medication by mouth with food as directed by your doctor, usually 2 times daily (within 1 hour after the morning and evening meal). Swallow the tablets whole. Do not crush, chew, or split the tablets. Doing so can release all of the drug at once, increasing the risk of side effects.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day. Keep taking this medication even if you feel well. Do not increase your dose, use this drug more often, or stop using it without first consulting your doctor.Get medical help right away if your asthma symptoms worsen or if you are using your quick-relief inhaler more than usual or more often than prescribed.
SIDE EFFECTS: Nausea or diarrhea may occur. If either of these effects lasts or gets worse, tell your doctor or pharmacist promptly.Remember that this medication has been prescribed because your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: symptoms of liver disease (such as nausea/vomiting that doesn't stop, loss of appetite, stomach/abdominal pain, yellowing eyes/skin, dark urine), mental/mood changes (such as trouble sleeping, agitation, hallucinations, depression, thoughts of suicide).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking zileuton, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, alcohol use.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Older women may be at greater risk for liver problems while using this drug.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this medication passes into breast milk. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.This medication can slow down the removal of other medications from your body, which may affect how they work. An example of an affected drug is pimozide, among others.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.
NOTES: Do not share this medication with others.Lab and/or medical tests (such as liver/lung function) should be done while you are taking this medication. Keep all medical and lab appointments. Consult your doctor for more details.Avoid substances that can worsen breathing problems by causing irritation or allergic reaction, such as smoke, pollen, pet dander, dust, and mold.
MISSED DOSE: If you miss a dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from light and moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
MEDICAL ALERT: Your condition can cause complications in a medical emergency. For information about enrolling in MedicAlert, call 1-888-633-4298 (US) or 1-800-668-1507 (Canada).
Information last revised August 2021. Copyright(c) 2022 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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