Fluconazole with Tipranavir Interaction Details
Brand Names Associated with Fluconazole
- Diflucan®
- Fluconazole
Brand Names Associated with Tipranavir
- Aptivus®
- Tipranavir
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Nov 27, 2023
Interaction Effect
Increased tipranavir exposure
Interaction Summary
Coadministered tipranavir/ritonavir and fluconazole may increase serum concentrations of tipranavir due to fluconazole inhibition of CYP3A4. Dose adjustments are not necessary; however, fluconazole doses greater than 200 mg per day are not recommended. Concomitant use of these two medications has no clinically-relevant effect on the plasma concentrations of fluconazole. Fluconazole-mediated CYP3A4 inhibition continues for 4 to 5 days after discontinuation because of the long half-life. Use caution with the coadministration of fluconazole and tipranavir and carefully monitor .
Severity
Major
Onset
Unspecified
Evidence
Established
How To Manage Interaction
Use caution with the coadministration of fluconazole and tipranavir. Administration of fluconazole with tipranavir may increase tipranavir plasma concentrations. A dose adjustment is not needed, however, concomitant use of fluconazole doses greater than 200 mg per day are not recommended. Monitor for tipranavir toxicity including increased levels of lipid profiles and increased levels of liver function tests, nausea, vomiting or diarrhea, fatigue, headache, and rash . Fluconazole-mediated CYP3A4 inhibition continues for 4 to 5 days after discontinuation because of the long half-life .
Mechanism Of Interaction
Inhibition of CYP3A4-mediated metabolism of tipranavir
Literature Reports
A) A study demonstrated the coadministration of tipranavir/ritonavir (TPV/RTV) with fluconazole increased the plasma concentrations of tipranavir. In the study, healthy subjects (n=20) received TPV/RTV 500 mg/200 mg twice daily to steady state with one fluconazole 200-mg loading dose on day 1 followed by 12 doses of fluconazole 100 mg once daily. Pharmacokinetic parameters were compared to historical data (n=68) and presented as the ratio of TPV/RTV plus fluconazole to TPV/RTV alone (90% CI). The ratios of Cmax, AUC, and Cmin of tipranavir all showed an increase with results of 1.32 (range 1.18 to 1.47), 1.5 (range 1.29 to 1.73), and 1.69 (range 1.33 to 2.09), respectively. A second study determined that the coadministration of TPV/RTV and fluconazole does not impact the plasma concentrations of fluconazole. Geometric mean ratios (GMR) for the pharmacokinetic parameters of fluconazole demonstrated no clinically-relevant effect on fluconazole plasma concentration with an AUC GMR of 0.92 (90% CI, 0.88 to 0.95), Cmax GMR of 0.94 (90% CI, 0.91 to 0.98), and Cmin GMR of 0.89 (90% CI, 0.85 to 0.92) .
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.
Tipranavir Overview
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Tipranavir is used with ritonavir (Norvir) and other medications to treat human immunodeficiency virus infection (HIV). Tipranavir is in a class of medications called protease inhibitors. It works by decreasing the amount of HIV in the blood. Although tipranavir does not cure HIV, it may decrease your chance of developing acquired immunodeficiency syndrome (AIDS) and HIV-related illnesses such as serious infections or cancer. Taking these medications along with practicing safer sex and making other lifestyle changes may decrease the risk of transmitting the HIV virus to other people.
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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.