Uses of Zileuton

Zileuton is used to prevent asthma symptoms, including shortness of breath, wheezing, coughing, and tightness in the chest. It does not treat asthma attacks that have already started. Zileuton is a leukotriene synthesis inhibitor, meaning that it stops the production of natural substances that cause tightening, swelling, and mucus production in the airways.

Side Effects Of Zileuton

Zileuton may cause side effects. Contact your physician if any of these are severe or persist:

  • diarrhea
  • headache
  • heartburn
  • irritation of the nose or throat
  • muscle pain
  • pain or swelling in the face

Some side effects can be serious. If you experience any of the following, seek treatment immediately:

  • dark urine
  • extreme fatigue
  • flu-like symptoms
  • itching
  • nausea or vomiting
  • rash/hives
  • stomach pain
  • yellowing of the eyes or skin

Warnings & Precautions

Before taking zileuton:

  • tell your doctor and pharmacist if you have any medication allergies, including to zileuton.
  • tell your doctor and pharmacist about any medications (prescription or over-the-counter) and supplements you are taking. It is especially important to mention the following: anticoagulants (blood thinners) [e.g., warfarin (Coumadin)]; antifungals [e.g., (Sporanox), ketoconazole (Nizoral)]; beta blockers [e.g., atenolol (Tenormin), labetalol (Trandate), metoprolol (Lopressor, Toprol XL), nadolol (Corgard), propranolol (Inderal)]; calcium channel blockers such as amlodipine (Norvasc), felodipine, isradipine (DynaCirc), nicardipine (Cardene), nifedipine (Adalat, Procardia), nimodipine, nisoldipine (Sular)]; cisapride (Propulsid); clarithromycin (Biaxin); cyclosporine (Gengraf, Neoral, Sandimmune); HIV protease inhibitors [e.g., atazanavir (Reyataz), indinavir (Crixivan), nelfinavir (Viracept), ritonavir (Norvir, in Kaletra), saquinavir (Invirase)]; nefazodone; telithromycin (Ketek); and theophylline (Theo-24, Uniphyl).
  • tell your doctor if you have or have had liver disease.
  • tell your doctor if you have difficulty swallowing pills or tablets.
  • tell your doctor if you consume or used to consume large quantities of alcohol. Ask about the safe use of alcohol while taking zileuton.
  • tell your doctor if you plan/desire to become pregnant, are pregnant, or are breast-feeding. Call your doctor immediately if you become pregnant while taking zileuton.
  • you should know that zileuton may cause changes in your mental health. Seek treatment immediately if you experience agitation, aggressiveness, anxiety, depression, difficulty sleeping, hallucinations, irritability, restlessness, suicidal thoughts or behaviors, tremors, or unusual dreams. Your doctor may advise you to discontinue using zileuton.

Dosage Of Zileuton

Zileuton comes in both a stand tablet and an extended-release tablet to be taken orally. The standard tablet is often taken four times a day, while the extended-release version is taken only twice a day (usually within an hour of morning and evening meals). Always take your medication exactly as prescribed.

Do not chew, crush, or split extended-release tablets.

Zileuton is not intended to treat sudden asthma attacks. Ask your doctor to prescribe a short-acting inhaler instead.

Do not discontinue other medications prescribed to treat your asthma. Tell your doctor if your asthma worsens while taking zilueton.

It may take several days for you feel the effects of zileuton. Continue to take your medication even if you feel fine.


Keep all appointments with your doctor and laboratory, as certain tests may be required before and during treatment.