Ketoconazole with Aripiprazole Lauroxil Interaction Details
Brand Names Associated with Ketoconazole
- Ketoconazole
- Nizoral®
Brand Names Associated with Aripiprazole Lauroxil
- Abilify Mycite®
- Abilify®
- Aripiprazole
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Dec 02, 2023
Interaction Effect
Increased aripiprazole exposure
Interaction Summary
Aripiprazole lauroxil is a prodrug of aripiprazole, and aripiprazole is a CYP3A4 substrate. Coadministration of aripiprazole lauroxil and a strong CYP3A4 inhibitor for longer than 2 weeks may result in increased aripiprazole exposure and increased risk of toxicity. If coadministration with Aristada(R) is required, reduce Aristada(R) to next lower strength (882 mg every 6 weeks or 1064 mg every 2 months is reduced to 441 mg monthly); a 441 mg monthly dosage may be continued if tolerated. Avoid concomitant use of a strong CYP3A4 inhibitor with Aristada Initio(TM) because the dosage of Aristada Initio(TM) cannot be modified .
Severity
Moderate
Onset
Unspecified
Evidence
Probable
How To Manage Interaction
Coadministration of aripiprazole lauroxil and a strong CYP3A4 inhibitor for longer than 2 weeks may result in increased aripiprazole exposure and increased risk of toxicity. If coadministration with Aristada(R) is required, reduce Aristada(R) to next lower strength (882 mg every 6 weeks or 1064 mg every 2 months is reduced to 441 mg monthly); a 441 mg monthly dosage may be continued if tolerated. Avoid concomitant use of a strong CYP3A4 inhibitor with Aristada Initio(TM) because the dosage of Aristada Initio(TM) cannot be modified .
Mechanism Of Interaction
Inhibition of CYP3A4-mediated metabolism of aripiprazole
Literature Reports
A) During drug interaction studies, coadministration of ketoconazole 200 mg/day for 14 days with a single oral dose of aripiprazole 15 mg resulted in a 63% and 77% increase in the AUC of aripiprazole and its active metabolite, respectively. Studies have not yet been conducted with higher ketoconazole doses (ie, 400 mg/day) .
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.
Aripiprazole Lauroxil Overview
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Aripiprazole is used to treat the symptoms of schizophrenia (a mental illness that causes disturbed or unusual thinking, loss of interest in life, and strong or inappropriate emotions) in adults and teenagers 13 years of age and older. It is also used alone or with other medications to treat episodes of mania or mixed episodes (symptoms of mania and depression that happen together) in adults, teenagers, and children 10 years of age and older with bipolar disorder (manic-depressive disorder; a disease that causes episodes of depression, episodes of mania, and other abnormal moods). Aripiprazole is also used with an antidepressant to treat depression when symptoms cannot be controlled by the antidepressant alone. Aripiprazole is also used to treat children 6 to 17 years of age who have autistic disorder (a developmental problem that causes difficulty communicating and interacting with others). Aripiprazole may help control irritable behavior such as aggression, temper tantrums, and frequent mood changes in these children. Aripiprazole is also used to treat children 6 to 18 years of age who have Tourette's disorder (a condition characterized by the need to perform repeated motions or to repeat sounds or words). Aripiprazole is in a class of medications called atypical antipsychotics. It works by changing the activity of certain natural substances in the brain.
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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.