Fluconazole with Lomitapide Interaction Details
Brand Names Associated with Fluconazole
- Diflucan®
- Fluconazole
Brand Names Associated with Lomitapide
- Juxtapid®
- Lomitapide
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Nov 27, 2023
Interaction Effect
Increased exposure of lomitapide
Interaction Summary
Concomitant use of lomitapide (a CYP3A4 substrate) with a moderate CYP3A4 inhibitor is contraindicated, as coadministration may result in significantly increased exposure of lomitapide. Although the interaction between lomitapide and moderate CYP3A4 inhibitors has not been studied, the concomitant use of a strong CYP3A4 inhibitor (ketoconazole 200 mg twice daily for 9 days) with lomitapide (60 mg daily) resulted in a 27-fold increase in lomitapide AUC and a 15-fold increase in lomitapide Cmax. One patient had markedly elevated transaminases (ie, ALT and AST) within days of initiating clarithromycin, a strong CYP3A4 inhibitor, during lomitapide clinical trials. If treatment with a moderate CYP3A4 inhibitor is unavoidable, discontinue lomitapide during the course of treatment.
Severity
Contraindicated
Onset
Unspecified
Evidence
Theoretical
How To Manage Interaction
The concomitant use of lomitapide, a CYP3A4 substrate, with a moderate CYP3A4 inhibitor is contraindicated. If treatment with a moderate CYP3A4 inhibitor is unavoidable, discontinue lomitapide during the course of treatment.
Mechanism Of Interaction
Inhibition of CYP3A4-mediated lomitapide metabolism
Literature Reports
A) During lomitapide clinical trials, a patient with homozygous familial hypercholesterolemia (HoFH) had markedly elevated transaminases (ALT, 24 times ULN; AST, 13 times ULN) within days of initiating clarithromycin, a strong CYP3A4 inhibitor .
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.
Lomitapide Overview
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Lomitapide is used along with diet changes (restriction of cholesterol and fat intake) and other treatments to reduce the amount of low-density lipoprotein (LDL) cholesterol ('bad cholesterol'), total cholesterol, and other fatty substances in the blood in people that have homozygous familial hypercholesterolemia (HoFH; an inherited condition in which cholesterol cannot be removed from the body normally). Lomitapide should not be used to decrease cholesterol levels in people who do not have HoFH. Lomitapide is in a class of medications called cholesterol-lowering medications. It works by slowing the production of cholesterol in the body to decrease the amount of cholesterol that may build up on the walls of the arteries and block blood flow to the heart, brain, and other parts of the body.
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Accumulation of cholesterol and fats along the walls of your arteries (a process known as atherosclerosis) decreases blood flow and, therefore, the oxygen supply to your heart, brain, and other parts of your body. Lowering your blood level of cholesterol and fats may help prevent heart disease, angina (chest pain), strokes, and heart attacks.
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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.