Drug interactions
Tizanidine + Zileuton
Severity: Major
Tizanidine and Zileuton: major interaction.
Last updated
For healthcare professionals — reference only. This page is a brief summary, not medical advice and not a substitute for official labeling or clinical judgement. Always verify before prescribing or dispensing.
Summary
Tizanidine is cleared mainly by CYP1A2 and is highly sensitive to inhibitors, which can cause marked hypotension, bradycardia and sedation. Zileuton is a weak CYP1A2 inhibitor but has been reported to raise tizanidine exposure, and the combination is cautioned in labeling.
What this interaction means in plain words
Tizanidine and Zileuton can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for.
Tizanidine belongs to Musculoskeletal; Zileuton belongs to Respiratory.
Why it happens
Zileuton inhibits CYP1A2, decreasing tizanidine clearance and increasing exposure.
What to do
Avoid the combination if possible. If both are required, start tizanidine at a low dose, titrate slowly and monitor blood pressure, heart rate and sedation.
What to ask your pharmacist
- Does the benefit of taking both outweigh the risk in my case?
- Do I need any blood test, ECG or other check while on both?
- What early warning signs should I watch for, and what should I do if they appear?
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Other interactions of Zileuton
- Fezolinetant + Zileuton Contraindicated
- Pimozide + Zileuton Contraindicated
- Alosetron + Zileuton Major
- Clozapine + Zileuton Major
- Lomitapide + Zileuton Major
- Lonafarnib + Zileuton Major
Other interactions of Tizanidine
- Ciprofloxacin + Tizanidine Contraindicated
- Fluvoxamine + Tizanidine Contraindicated
- Pefloxacin + Tizanidine Contraindicated
- Pipemidic acid + Tizanidine Contraindicated
- Benzhydrocodone / acetaminophen + Tizanidine Major
- Brexanolone + Tizanidine Major
Frequently asked questions
Can I take Tizanidine with Zileuton?
MediHelp rates the interaction as major. Tizanidine and Zileuton can interact in a way that may be serious. Using them together is sometimes necessary, but it needs a deliberate decision by the prescriber, a plan for monitoring, and clear advice on the warning signs to watch for. Tizanidine is cleared mainly by CYP1A2 and is highly sensitive to inhibitors, which can cause marked hypotension, bradycardia and sedation. Zileuton is a weak CYP1A2 inhibitor but has been reported to raise tizanidine exposure, and the combination is cautioned in labeling.
How serious is the interaction between Tizanidine and Zileuton?
MediHelp rates it major, on a four-level scale (minor, moderate, major, contraindicated) based on published labels and references. What to do, in brief: Avoid the combination if possible. If both are required, start tizanidine at a low dose, titrate slowly and monitor blood pressure, heart rate and sedation.
What other medicines interact with Zileuton?
MediHelp also lists interactions of Zileuton with, for example, Fezolinetant, Pimozide, Alosetron. The full list is on the Zileuton page.
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