Fluconazole with Etrasimod Interaction Details
Brand Names Associated with Fluconazole
- Diflucan®
- Fluconazole
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Nov 27, 2023
Interaction Effect
Increased etrasimod exposure, increased risk of transient decrease in heart rate, AV conduction, QT interval prolongation and torsade de pointes
Interaction Summary
Fluconazole is a moderate CYP3A4 inhibitor that has been associated with prolongation of the QT interval and torsade de pointes. Coadministration of fluconazole with CYP3A4 substrates that are known to prolong the QT interval is contraindicated. Fluconazole-mediated CYP3A4 inhibition may continue for 4 to 5 days after discontinuation because of the long half-life. Concomitant use of etrasimod with a drug that is a moderate to strong inhibitor of CYP2C9 and a moderate to strong inhibitor of CYP3A4 such as fluconazole is not recommended due to the potential for increased exposure of etrasimod. In a drug interaction study, concomitant use of etrasimod with steady-state fluconazole increased etrasimod AUC by 84%. Also, a transient decrease in heart rate and AV conduction delays may occur when initiating etrasimod. Because of the potential additive effect on heart rate, etrasimod may increase the risk of QT prolongation and torsades de pointes with concomitant use of QT prolonging drugs. Seek the advice of a cardiologist before initiating etrasimod treatment with other drugs that prolong the QT interval .
Severity
Contraindicated
Onset
Unspecified
Evidence
Probable
How To Manage Interaction
Fluconazole is a moderate CYP3A4 inhibitor that has been associated with prolongation of the QT interval and torsade de pointes. Coadministration of fluconazole with CYP3A4 substrates that are known to prolong the QT interval is contraindicated. Fluconazole-mediated CYP3A4 inhibition may continue for 4 to 5 days after discontinuation because of the long half-life. Concomitant use of etrasimod with a drug that is a moderate to strong inhibitor of CYP2C9 and a moderate to strong inhibitor of CYP3A4 such as fluconazole is not recommended due to the potential for increased exposure of etrasimod. Also, a transient decrease in heart rate and AV conduction delays may occur when initiating etrasimod. Because of the potential additive effect on heart rate, etrasimod may increase the risk of QT prolongation and torsades de pointes with concomitant use of QT prolonging drugs. Seek the advice of a cardiologist before initiating etrasimod treatment with other drugs that prolong the QT interval .
Mechanism Of Interaction
Inhibition of CYP3A4-mediated metabolism of etrasimod; inhibition of CYP2C9-mediated metabolism of etrasimod; additive heart rate reduction and QT interval prolongation
Literature Reports
A) In a drug interaction study, concomitant use of etrasimod with steady-state fluconazole (a moderate CYP2C9 and a CYP3A4 inhibitor) increased etrasimod AUC by 84% .
Fluconazole Overview
-
Fluconazole is used to treat fungal infections, including yeast infections of the vagina, mouth, throat, esophagus (tube leading from the mouth to the stomach), abdomen (area between the chest and waist), lungs, blood, and other organs. Fluconazole is also used to treat meningitis (infection of the membranes covering the brain and spine) caused by fungus. Fluconazole is also used to prevent yeast infections in patients who are likely to become infected because they are being treated with chemotherapy or radiation therapy before a bone marrow transplant (replacement of unhealthy spongy tissue inside the bones with healthy tissue). Fluconazole is in a class of antifungals called triazoles. It works by slowing the growth of fungi that cause infection.
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Definitions
Severity Categories
Contraindicated
These drugs, generally, should not be used together simultaneously due to the high risk of severe adverse effects. Combining these medications can lead to dangerous health outcomes and should be strictly avoided unless otherwise instructed by your provider.
Major
This interaction could result in very serious and potentially life-threatening consequences. If you are taking this drug combination, it is very important to be under close medical supervision to minimize severe side effects and ensure your safety. It may be necessary to change a medication or dosage to prevent harm.
Moderate
This interaction has the potential to worsen your medical condition or alter the effectiveness of your treatment. It's important that you are monitored closely and you potentially may need to make adjustments in your treatment plan or drug dosage to maintain optimal health.
Minor
While this interaction is unlikely to cause significant problems, it could intensify side effects or reduce the effectiveness of one or both medications. Monitoring for changes in symptoms and your condition is recommended, and adjustments may be made if needed to manage any increased or more pronounced side effects.
Onset
Rapid: Onset of drug interaction typically occurs within 24 hours of co-administration.
Delayed: Onset of drug interaction typically occurs more than 24 hours after co-administration.
Evidence
Level of documentation of the interaction.
Established: The interaction is documented and substantiated in peer-reviewed medical literature.
Theoretical: This interaction is not fully supported by current medical evidence or well-documented sources, but it is based on known drug mechanisms, drug effects, and other relevant information.
How To Manage The Interaction
Provides a detailed discussion on how patients and clinicians can approach the identified drug interaction as well as offers guidance on what to expect and strategies to potentially mitigate the effects of the interaction. This may include recommendations on adjusting medication dosages, altering the timing of drug administration, or closely monitoring for specific symptoms.
It's important to note that all medical situations are unique, and management approaches should be tailored to individual circumstances. Patients should always consult their healthcare provider for personalized advice and guidance on managing drug interactions effectively.
Mechanism Of Interaction
The theorized or clinically determined reason (i.e., mechanism) why the drug-drug interaction occurs.
Disclaimer: The information provided on this page is for informational purposes only and should not be considered medical advice. Always consult with a qualified healthcare professional regarding your specific circumstances and medical conditions.
Where Does Our Information Come From?
Information for our drug interactions is compiled from several drug compendia, including:
The prescribing information for each drug, as published on DailyMED, is also used.
Individual drug-drug interaction detail pages contain references specific to that interaction. You can click on the reference number within brackets '[]' to see what reference was utilized.
The information posted is fact-checked by HelloPharmacist clinicians and reviewed quarterly.