A drug that inhibits leukotriene formation, reduces the inflammatory process, and is used in the treatment of asthma.
[zi- (perhaps shortening and alteration of ENZYME) + LEU(KO)T(RIENE) + –ON3.]
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A drug that inhibits leukotriene formation, reduces the inflammatory process, and is used in the treatment of asthma.
[zi- (perhaps shortening and alteration of ENZYME) + LEU(KO)T(RIENE) + –ON3.]
Brand names: Zyflo®
Chemical formula:

Zileuton tablets
What are zileuton tablets?
Zileuton (Zyflo®) is used to treat asthma. It helps to reduce recurring symptoms of asthma, but it is not for rapid relief of asthma attacks. Generic zileuton tablets are not available.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
liver disease
a history of alcoholism
fever or infection
an unusual or allergic reaction to zileuton, other medicines, foods, dyes, or preservatives
pregnant or trying to get pregnant
breast-feeding
How should I take this medicine?
Take zileuton tablets by mouth. Follow the directions on the prescription label. Take your doses at regular intervals. Zileuton may be taken with meals and at bedtime. Do not take your medicine more often than directed.
Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses.What drug(s) may interact with zileuton?
alosetron
astemizole
bosentan
caffeine
carbamazepine
certain drugs for anxiety, insomnia, or difficulty sleeping (such as alprazolam, diazepam, midazolam, or triazolam)
certain drugs used to lower cholesterol (atorvastatin, cerivastatin, lovastatin, simvastatin)
certain drugs used for HIV infection or AIDS (such as indinavir, ritonavir, or saquinavir)
certain heart or high blood pressure medicines (such as bepridil, diltiazem, felodipine, lidocaine, nicardipine, nifedipine, nimodipine, nisoldipine, propranolol, quinidine, or verapamil)
cisapride
clarithromycin or erythromycin
cyclosporine
donepezil
doxercalciferol
ergot alkaloids (such as dihydroergotamine, ergotamine, methysergide or methylergonovine)
guarana
imatinib, STI-571
paricalcitol
pimozide
ramelteon
sirolimus
steroid drugs (such as prednisone, hydrocortisone, dexamethasone)
tacrolimus
terfenadine
theophylline or aminophylline
voriconazole
warfarin
went yeast
zonisamide
Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.
What should I watch for while taking zileuton?
It is important that you go on taking your medicine even when you do not have any asthma symptoms. Tell your prescriber or health care professional if your asthma symptoms do not start to improve after several days. Only stop taking zileuton on your prescriber's advice.
Visit your prescriber or health care professional for regular checks on your progress. Liver tests will need to be done on a regular basis while taking zileuton.
What side effects may I notice from taking zileuton?
Side effects that you should report to your prescriber or health care professional as soon as possible:
chest pain
difficulty breathing, wheezing
flu-like symptoms (chills, fatigue, fever, muscle aches)
nausea
pruritus
skin rash or itching
unusual weakness or tiredness
yellowing of the skin
Call your prescriber or health care professional immediately if you get any of these side effects.
Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
back pain
dizziness
drowsiness
dyspepsia
headache
insomnia
numbness or tingling in the hands or feet
stomach pain
weakness
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.
Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
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Zileuton
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| Systematic (IUPAC) name | |
| 1-(1-benzothiophen-2-ylethyl)-1-hydroxy-urea | |
| Identifiers | |
| CAS number | |
| ATC code | ? |
| PubChem | |
| DrugBank | |
| Chemical data | |
| Formula | C11H12N2O2S |
| Mol. mass | 236.291 g/mol |
| Pharmacokinetic data | |
| Bioavailability | Not yet established |
| Protein binding | 93% |
| Metabolism | Hepatic (CYP1A2, CYP2C9 and CYP3A4-mediated) |
| Half life | 2.5 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
C(US) |
| Legal status | |
| Routes | Oral |
Zileuton (INN) is an asthma drug. It blocks leukotriene synthesis by inhibiting 5-lipoxygenase, an enzyme of the eicosanoid synthesis pathway.
Zileuton is marketed by Critical Therapeutics under the brand name Zyflo®.
| Drugs for obstructive airway diseases: asthma/COPD (R03) | |
|---|---|
| Adrenergics, inhalants | Short
acting β2-agonists: Salbutamol/Levosalbutamol • Fenoterol • Terbutaline Long acting β2-agonists (LABA): Bambuterol • Clenbuterol • Formoterol • Salmeterol other: Epinephrine • Isoproterenol • Orciprenaline |
| Glucocorticoids | Beclometasone • Budesonide • Ciclesonide • Fluticasone • Mometasone |
| Anticholinergics | Ipratropium • Tiotropium |
| Mast cell stabilizers | Cromoglicate • Nedocromil |
| Xanthines | Aminophylline • Theobromine • Theophylline |
| Leukotriene antagonists | Montelukast • Pranlukast • Zafirlukast |
| Combination products | Budesonide/formoterol • Fluticasone/salmeterol • Ipratropium/salbutamol |
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Copyrights:
![]() | Dictionary. The American Heritage® Dictionary of the English Language, Fourth Edition Copyright © 2007, 2000 by Houghton Mifflin Company. Updated in 2007. Published by Houghton Mifflin Company. All rights reserved. Read more | |
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