Ketoconazole with Budesonide Interaction Details
Brand Names Associated with Ketoconazole
- Ketoconazole
- Nizoral®
Brand Names Associated with Budesonide
- Budesonide
- Entocort® EC
- Tarpeyo ®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 02, 2023
Interaction Effect
Increased budesonide exposure
Interaction Summary
Avoid use of budesonide delayed-release capsules with ketoconazole, a strong CYP3A4 inhibitor, as the exposure of budesonide may be increased. Use caution while considering the coadministration of budesonide with long-term ketoconazole. Concomitant administration of ketoconazole with budesonide may inhibit the metabolism of budesonide and may increase systemic budesonide exposure .
Severity
Major
Onset
Rapid
Evidence
Established
How To Manage Interaction
Avoid use of budesonide oral delayed-release capsules with ketoconazole, a strong CYP3A4 inhibitor, as the exposure of budesonide may be increased. Use caution while considering the coadministration of inhaled budesonide with long-term ketoconazole. Concomitant administration of ketoconazole with budesonide may inhibit the metabolism of budesonide and may increase systemic budesonide exposure .
Mechanism Of Interaction
Inhibition of CYP3A4-mediated metabolism of budesonide by ketoconazole
Literature Reports
A) In an open, nonrandomized, cross-over study, coadministration of budesonide and ketoconazole resulted in 8-fold the AUC of budesonide, compared to budesonide alone. Six healthy subjects were given budesonide 10 mg as a single dose, either alone or concomitantly with the last ketoconazole dose of 3 days treatment with ketoconazole 100 mg twice daily .
B) A randomized, open crossover study involving eight healthy volunteers demonstrated the effect of ketoconazole on the elimination of budesonide. In period 1, a single dose of budesonide 3 mg was given in the morning without ketoconazole pretreatment. In the second period, ketoconazole was administered once daily in the morning on four consecutive days. Budesonide 3 mg was administered with ketoconazole on the fourth day. In period three, ketoconazole was administered once daily in the evening for four consecutive days. On the fourth day, budesonide was administered twelve hours before the last dose of ketoconazole. A significant increase in plasma concentrations of budesonide was observed during morning and evening treatment with ketoconazole. The mean maximum plasma concentration (Cmax) of budesonide was increased by about 7.7 times and the mean AUC was increased by about 6.8 times when ketoconazole was administered with budesonide. The increase in the plasma concentration of budesonide was smaller when ketoconazole was administered twelve hours before budesonide. The mean Cmax of budesonide was increased by approximately 3.6 times and the mean AUC was increased by about 4 times .
Ketoconazole Overview
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Ketoconazole is used to treat fungal infections when other medications are not available or cannot be tolerated. Ketoconazole should not be used to treat fungal meningitis (infection of the membranes surrounding the brain and spinal cord caused by a fungus) or fungal nail infections. Ketoconazole is in a class of antifungals called imidazoles. It works by slowing the growth of fungi that cause infection.
Budesonide Overview
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Budesonide (Entocort EC) is used to treat Crohn's disease (a condition in which the body attacks the lining of the digestive tract, causing pain, diarrhea, weight loss, and fever). Budesonide (Tarpeyo) is used to decrease protein in the urine in patients with primary immunoglobulin A nephropathy (kidney disease that occurs in some people when too much immunoglobin A builds up in the kidney, causing inflammation). Budesonide is in a class of medications called corticosteroids. It works by decreasing inflammation (swelling) in the digestive tract of people who have Crohn's disease or in the kidney of people with nephropathy.
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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.