Buspirone with Itraconazole Interaction Details
Brand Names Associated with Buspirone
- BuSpar®
- Buspirone
Brand Names Associated with Itraconazole
- Itraconazole
- Onmel®
- Sporanox®
- Tolsura®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Mar 06, 2024
Interaction Effect
Increased busPIRone exposure and increased busPIRone-related side effects (impaired psychomotor performance, sedation)
Interaction Summary
Concomitant use of itraconazole with busPIRone may increase the concentrations of busPIRone resulting in an increased risk of busPIRone-related adverse reactions. Monitor for adverse reactions of busPIRone. BusPIRone dose reduction may be necessary[1]. Peak plasma concentrations and bioavailability of busPIRone were significantly increased by itraconazole in eight healthy females in a double blind randomized study [2]. If concomitant administration of busPIRone and itraconazole is necessary, low doses of busPIRone (2.5 mg twice daily) should be utilized and further dosing adjustments should be based on clinical assessment [3]. Significant increases in plasma concentrations of busPIRone occurs when coadministered with itraconazole [4].
Severity
Major
Onset
Rapid
Evidence
Probable
How To Manage Interaction
Concomitant use of itraconazole with busPIRone may increase the concentrations of busPIRone resulting in an increased risk of busPIRone-related adverse reactions. Monitor for adverse reactions of busPIRone. BusPIRone dose reduction may be necessary[1].
Mechanism Of Interaction
Inhibition of CYP3A4-mediated metabolism of busPIRone by itraconazole
Literature Reports
A) Peak plasma concentrations and bioavailability of busPIRone were significantly increased by itraconazole in eight healthy females in a double blind randomized study. Patients were randomized to receive either itraconazole 100 mg two times daily or placebo for four days. On the fourth day a single dose of busPIRone 10 mg was given with the last dose of itraconazole. Compared to placebo, the average peak plasma level of busPIRone was increased from 1 ng/mL to 13.4 ng/mL (3 nanomoles/L to 34.8 nanomoles/L) by itraconazole. The average area under the plasma concentration time curve from time zero to infinity was increased from 3.3 ng/mL h for placebo, to 63.2 ng/mL h with itraconazole. The elimination half-life of busPIRone was not effected by itraconazole. This may be because the itraconazole was discontinued when the busPIRone was given. Performance in psychomotor tests was significantly impaired in subjects receiving both itraconazole and busPIRone, compared to subjects receiving busPIRone and placebo. Itraconazole should be avoided in patients treated with busPIRone [2].
References
1 ) Product Information: SPORANOX(R) oral capsules, itraconazole oral capsules. Janssen Pharmaceuticals Inc (per FDA), Titusville, NJ, 2022.
2 ) Kivisto KT, Lamberg TS, Kantola T, et al: Plasma buspirone concentrations are greatly increased by erythromycin and itraconazole. Clin Pharmacol Ther 1997; 86:348-354.
3 ) Product Information: BuSpar(R), buspirone. Bristol-Myers Squibb Company, Princeton, NJ, 1998.
4 ) Product Information: Sporanox(R), itraconazole. Janssen Pharmaceutica Products, L.P., Titusville, New Jersey, 2002.
Buspirone Overview
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Buspirone is used to treat anxiety disorders or in the short-term treatment of symptoms of anxiety. Buspirone is in a class of medications called anxiolytics. It works by changing the amounts of certain natural substances in the brain.
Itraconazole Overview
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Itraconazole capsules (Sporanox, Tolsura) are used to treat fungal infections in the lungs that can spread throughout the body. Itraconazole capsules (Sporanox) are also used to treat fungal infections of the fingernails and toenails. Itraconazole oral solution (liquid) is used to treat yeast infections of the mouth and throat or of the esophagus (tube that connects the throat to the stomach). Itraconazole 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.