Fluconazole with Triazolam Interaction Details
Brand Names Associated with Fluconazole
- Diflucan®
- Fluconazole
Brand Names Associated with Triazolam
- Halcion®
- Triazolam
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Nov 27, 2023
Interaction Effect
Increased triazolam exposure and an increased risk of triazolam-related toxicity (excessive sedation and prolonged hypnotic effects)
Interaction Summary
Concomitant administration of these two agents is not recommended. Fluconazole increases the AUC of triazolam (single dose) by approximately 50%, Cmax by 20% to 32%, and increases half-life by 25% to 50 % due to the inhibition of metabolism of triazolam. Dosage adjustments of triazolam may be necessary .
Severity
Major
Onset
Rapid
Evidence
Established
How To Manage Interaction
Concomitant administration of fluconazole with triazolam may increase the concentrations of triazolam due to inhibition of metabolism of triazolam. Dosage adjustments of triazolam may be necessary.
Mechanism Of Interaction
Inhibition of CYP3A4-mediated metabolism of triazolam by fluconazole
Literature Reports
A) In a double-blind, randomized, cross-over study of four phases, eight healthy volunteers received fluconazole 50 mg, 100 mg, or 200 mg (400 mg on day 1) or placebo orally every day for four days. Subjects were given one dose of triazolam 0.25 mg on day 4. Plasma samples were obtained and the pharmacodynamic effects were determined for 18 hours. Fluconazole 50 mg, 100 mg, and 200 mg increased the mean area under the concentration-time curve (AUC) of triazolam 1.6-, 2.1- and 4.4-fold, respectively. During all fluconazole phases, the peak concentration of triazolam was increased significantly, and the elimination half-life was increased from 1.3-fold to 2.3-fold. Fluconazole 100 mg and 200 mg also significantly increased the pharmacodynamic effects of triazolam .
B) Studies have shown fluconazole to be a inhibitor of cytochrome P450 3A (CYP3A) enzymes, an enzyme subfamily thought to be important in triazolam metabolism . Because the initial step in triazolam metabolism is hydroxylation catalyzed by CYP3A, fluconazole may have a profound effect on the clearance of triazolam .
C) Fluconazole increases the AUC of triazolam (single dose) by approximately 50%, Cmax by 20% to 32%, and increases half-life by 25% to 50 % due to the inhibition of metabolism of triazolam .
Fluconazole Overview
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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.
Triazolam Overview
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Triazolam is used on a short-term basis to treat insomnia (difficulty falling asleep or staying asleep). Triazolam is in a class of medications called benzodiazepines. It works by slowing activity in the brain to allow sleep.
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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.