Zileuton

Zileuton is a prescription medicine used for the prophylaxis and chronic treatment of asthma in adults and children 12 years of age and older.

• Zileuton is available under the following different brand names: Zyflo Filmtab, Zyflo, Zyflo CR.

Common side effects of Zileuton include:

• stuffy nose
• sinus pain
• sneezing
• sore throat
• headache
• diarrhea
• upset stomach
• weakness
• muscle pain

Serious side effects of Zileuton include:

• hives
• difficulty breathing
• swelling of the face, lips, tongue, or throat
• nausea
• upper stomach pain
• itching
• loss of appetite
• dark urine
• clay-colored stools
• yellowing of the skin or eyes (jaundice)
• skin rash
• bruising
• severe tingling
• numbness
• pain
• muscle weakness
• mood or behavior changes
• anxiety
• depression
• thoughts about suicide or hurting oneself
• worsening asthma symptoms

Rare side effects of Zileuton include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, coordination loss, unsteady, very stiff muscles, high fever, profuse sweating, or tremors.
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights.
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out.

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Tablet

• 600 mg

Tablet, extended-release.

• 600 mg

Asthma

Adult dosage

• Extended-release: 1200 mg orally twice daily, within 1 hour after morning and evening meals
• Conventional: 600 mg orally four times daily

Pediatric dosage

• Children under 12 years
  • Safety and efficacy not established.
  • The FDA has not required pediatric studies in patients under 12 years old due to the risk of hepatotoxicity; not recommended for children younger than 12 years.
• Children above 12 years
  • Extended Release: 1200 mg orally twice daily, within 1 hour after morning and evening meals.
  • Conventional: 600 mg orally four times daily.

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Zileuton has severe interactions with the following drugs:
  • fezolinetant
  • flibanserin
• Zileuton has serious interactions with the following drugs:
  • alosetron
  • cobimetinib
  • duloxetine
  • eliglustat
  • fentanyl
  • fentanyl intranasal
  • fentanyl transdermal
  • fentanyl transmucosal
  • irinotecan liposomal
  • ivabradine
  • lonafarnib
  • naloxegol
  • olaparib
  • pimozide
  • pirfenidone
  • tizanidine
• Zileuton has moderate interactions with at least 40 other drugs.
• Zileuton has minor interactions with the following drugs:
  • antipyrine
  • asenapine
  • caffeine
  • frovatriptan
  • ondansetron
  • riluzole

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all the products you use. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, health questions, or concerns.

Contraindications

• hypersensitivity
• liver disease, LFTs 3×ULN or more

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Zileuton?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Zileuton?”

Cautions

• Not indicated for use in acute bronchospasm
• History of liver disease, and heavy alcohol use
• Behavioral changes and sleep disorders reported
• Not recommended for patients less than 12 years due to the risk of hepatotoxicity

Pregnancy and Lactation

• There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to asthma medications during pregnancy; for more information, contact the Mother to Baby Pregnancy Studies conducted by the 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
• 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 the effects of a drug on breastfed infants 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 the breastfed child from the drug or from the underlying maternal condition