Zileuton

Name: Zileuton Drug Interactions
Creator: Dr. Brian Staiger, PharmD, BCPS

12 interactions

Also sold as: Zyflo Zyflo® Zyflo® CR

About Zileuton

Zileuton is used to prevent wheezing, shortness of breath, coughing, and chest tightness due to asthma. Zileuton is not used to treat an asthma attack (sudden episode of shortness of breath, wheezing, and coughing) that has already started. Zileuton belongs to a class of medications called leukotriene synthesis inhibit… Read the full Zileuton drug information page →

Medically reviewed by Dr. Brian Staiger, PharmD, BCPS · Updated Jun 30, 2026 · Editorial policy · Data sources

Sources: FDA prescribing information (Structured Product Labeling), the published literature cited in each entry, DDInter 2.0 (a major open-access drug-interaction database), and legacy DrugBank interaction data distributed by the NIH's RxNav service (decommissioned in 2024) — analyzed and reviewed by our pharmacist team. How we build this library →

Most serious with: Anagrelide Dihydroergotamine Injection Dihydroergotamine Nasal Spray Methylergonovine

4 Major 8 Moderate

All (12) Major (4) Moderate (8)

Major

Zileuton Anagrelide Agrylin Increased anagrelide exposure Details Zileuton Dihydroergotamine Injection DHE-45® Injection Increased ergot derivatives exposure and an increased risk of ergotism (nausea, vomiting, vasospastic ischemia) Details Zileuton Dihydroergotamine Nasal Spray Migranal Increased ergot derivatives exposure and an increased risk of ergotism (nausea, vomiting, vasospastic ischemia) Details Zileuton Methylergonovine Methergine Increased ergot derivatives exposure and an increased risk of ergotism (nausea, vomiting, vasospastic ischemia) Details

Moderate

Zileuton Betaxolol Betoptic S A significant increase in beta-adrenergic blockade Details Zileuton Betaxolol Ophthalmic Betoptic® A significant increase in beta-adrenergic blockade Details Zileuton Bisoprolol Zebeta® A significant increase in beta-adrenergic blockade Details Zileuton Ketoconazole Topical Extina® Foam Increased zileuton plasma concentrations Details Zileuton Labetalol Normodyne® A significant increase in beta-adrenergic blockade Details Zileuton Levobunolol Ophthalmic AKBeta® A significant increase in beta-adrenergic blockade Details Zileuton Nebivolol Bystolic A significant increase in beta-adrenergic blockade Details Zileuton Penbutolol Levatol® A significant increase in beta-adrenergic blockade Details

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Educational information only, not medical advice. Always confirm interactions with your pharmacist or prescriber before making any change to your medications.