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Zileuton

Also known as: Zyflo

5-Lipoxygenase Inhibitor5-Lipoxygenase Inhibitors

Route: Oral

13 interactions on record

Zileuton has 13 known drug interactions based on U.S. FDA drug labeling data. 7 are classified as major interactions requiring close medical supervision. Notable interactions include combinations with Propranolol, Theophylline, Tizanidine. Patients taking Zileuton should inform their healthcare provider of all current medications — including over-the-counter drugs and supplements — to avoid potentially harmful combinations. Data sourced from OpenFDA and the NIH National Library of Medicine.

Total: 13
Major: 7
Moderate: 5

Major (7)

Zileuton + Propranolol— Zileuton significantly increases propranolol concentrations by decreasing clearance 42%, resulting in 52% increase in Cm…
Zileuton + Theophylline— Zileuton significantly decreases theophylline clearance (~50%), doubling AUC and increasing Cmax by 73%. Theophylline-re…
Zileuton + Tizanidine— CYP1A2 inhibitor; concomitant use should be avoided due to potential for hypotension, bradycardia, or excessive drowsine…
Zileuton + Tizanidine Hydrochloride— Concomitant use should be avoided due to potential interactions. If clinically necessary, initiate with 2 mg and titrate…
Zileuton + Tizanidne Hydrochloride— Should be avoided due to CYP1A2 inhibition. If necessary, initiate tizanidine at 2 mg and titrate cautiously; monitor fo…
Zileuton + Warfarin— Zileuton decreases R-warfarin clearance by 15% and increases AUC by 22%, resulting in clinically significant increases i…
Zileuton + Warfarin Sodium— CYP1A2 inhibitor that increases warfarin effect and INR; requires close monitoring.

Moderate (5)

Zileuton + Carbamazepine— CYP3A4 inhibitor that increases plasma levels of carbamazepine; dose adjustment and/or plasma level monitoring may be ne…
Zileuton + Dihydroergotamine Mesylate— Moderate CYP3A4 inhibitor; administer with caution due to potential vasospasm risk.
Zileuton + Methylergonovine Maleate— Less potent CYP 3A4 inhibitor; should be administered with caution due to potential vasospastic effects.
Zileuton + Propranolol Hydrochloride— CYP1A2 substrate/inhibitor that may increase blood levels and/or toxicity of propranolol.
Zileuton + Riluzole— CYP1A2 inhibitor that may increase riluzole exposure and risk of riluzole-associated adverse reactions.

Zileuton + Propranolol⚠️Major

Zileuton significantly increases propranolol concentrations by decreasing clearance 42%, resulting in 52% increase in Cmax and 104% increase in AUC. Enhanced β-blockade activity observed. Monitor closely and reduce propranolol dose as necessary.

Zileuton + Theophylline⚠️Major

Zileuton significantly decreases theophylline clearance (~50%), doubling AUC and increasing Cmax by 73%. Theophylline-related adverse reactions occur more frequently. Reduce theophylline dose by approximately one-half and monitor plasma concentrations.

Zileuton + Tizanidine⚠️Major

CYP1A2 inhibitor; concomitant use should be avoided due to potential for hypotension, bradycardia, or excessive drowsiness.

Zileuton + Tizanidine Hydrochloride⚠️Major

Concomitant use should be avoided due to potential interactions. If clinically necessary, initiate with 2 mg and titrate cautiously.

Zileuton + Tizanidne Hydrochloride⚠️Major

Should be avoided due to CYP1A2 inhibition. If necessary, initiate tizanidine at 2 mg and titrate cautiously; monitor for hypotension, bradycardia, or excessive drowsiness.

Zileuton + Warfarin⚠️Major

Zileuton decreases R-warfarin clearance by 15% and increases AUC by 22%, resulting in clinically significant increases in prothrombin times. Monitor prothrombin time and adjust warfarin dose accordingly.

Zileuton + Warfarin Sodium⚠️Major

CYP1A2 inhibitor that increases warfarin effect and INR; requires close monitoring.

Zileuton + Carbamazepine🟡Moderate

CYP3A4 inhibitor that increases plasma levels of carbamazepine; dose adjustment and/or plasma level monitoring may be necessary.

Zileuton + Dihydroergotamine Mesylate🟡Moderate

Moderate CYP3A4 inhibitor; administer with caution due to potential vasospasm risk.

Zileuton + Methylergonovine Maleate🟡Moderate

Less potent CYP 3A4 inhibitor; should be administered with caution due to potential vasospastic effects.

Zileuton + Propranolol Hydrochloride🟡Moderate

CYP1A2 substrate/inhibitor that may increase blood levels and/or toxicity of propranolol.

Zileuton + Riluzole🟡Moderate

CYP1A2 inhibitor that may increase riluzole exposure and risk of riluzole-associated adverse reactions.

Zileuton + Ketoconazoleℹ️Unknown

However, no formal drug-drug interaction studies between zileuton and CYP3A4 inhibitors, such as ketaconazole, have been conducted.

Data sourced from U.S. FDA drug labeling via openFDA and the NIH National Library of Medicine, supplemented with a small number of well-established interactions from curated clinical references. For informational purposes only. Always consult your pharmacist or physician.