Bexarotene with Methotrexate Interaction Details
Brand Names Associated with Bexarotene
- Bexarotene
- Targretin® Capsules
Brand Names Associated with Methotrexate
- Amethopterin
- Methotrexate
- MTX
- Rheumatrex®
- Trexall®
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Mar 04, 2024
Interaction Effect
An increased risk of hepatotoxicity, an increased methotrexate exposure, an increased risk of methotrexate-related severe adverse reactions, reduced active metabolite formation and possibly reduced methotrexate efficacy
Interaction Summary
Coadministration of methotrexate with hepatotoxic agents like bexarotene may increase methotrexate plasma concentrations, which may increase the risk of methotrexate severe adverse reactions. In some cases, the coadministration of methotrexate with bexarotene may also subsequently reduce active metabolite formation, which may decrease the clinical effectiveness of methotrexate. If coadministration cannot be avoided, monitor closely for methotrexate adverse reactions. Increased organ specific adverse reactions may also occur when methotrexate is coadministered with hepatotoxic products[1]. In a number of case reports, the concurrent use of methotrexate and etretinate , a retinoid, resulted in signs of hepatotoxicity within 1 to 4 weeks of treatment. Methotrexate has also been reported to increase the risk of hepatotoxicity by greater than 30%. Since both drugs are hepatotoxic, it is difficult to attribute this toxicity to their concurrent use [2][3][4][5][6][7][8][9][10].
Severity
Major
Onset
Delayed
Evidence
Theoretical
How To Manage Interaction
Coadministration of methotrexate with hepatotoxic agents like bexarotene may increase methotrexate plasma concentrations, which may increase the risk of methotrexate severe adverse reactions. In some cases, the coadministration of methotrexate with bexarotene may also subsequently reduce active metabolite formation, which may decrease the clinical effectiveness of methotrexate. If coadministration cannot be avoided, monitor closely for methotrexate adverse reactions. Increased organ specific adverse reactions may also occur when methotrexate is coadministered with hepatotoxic products[1].
Mechanism Of Interaction
Additive hepatotoxic effects, decreased methotrexate clearance
Literature Reports
A) In a number of case reports, the concurrent use of methotrexate and etretinate, a retinoid, resulted in signs of hepatotoxicity within 1 to 4 weeks of treatment. Methotrexate has also been reported to increase the risk of hepatotoxicity by greater than 30%. Since both drugs are hepatotoxic, it is difficult to attribute this toxicity to their concurrent use [2][3][4][5][6][7][8][9][10].
References
1 ) Product Information: Jylamvo(R) oral solution, methotrexate oral solution. Lukare Medical, LLC (per FDA), Scotch Plains, NJ, 2022.
2 ) Product Information: Soriatane(R), acetretin capsules. Roche Laboratories, Inc., Nutley, NJ, 2003.
3 ) Product Information: Methotrexate LPF(R), methotrexate. Xanodyne Pharmacal, Inc., Florence, KY, 2003.
4 ) Product Information: Vesanoid(R), tretinoin. Roche Laboratories, Nutley, NJ, 2003.
5 ) Product Information: Targretin(R), bexarotene. Ligand Pharmaceuticals, Inc., San Diego, CA, 2002.
6 ) Product Information: Accutane(R), isotretinoin. Roche Laboratories, Nutley, NJ, 2000.
7 ) Product Information: Tegison(R), etretinate. Roche Dermatologics, Little Falls, NJ, 1995.
8 ) Zachariae H: Methotrexate and etretinate as concurrent therapies in the treatment of psoriasis (letter). Arch Dermatol 1984; 120:155.
9 ) Zachariae H: Dangers of methotrexate/etretinate combination therapy (letter). Lancet 1988; 1:422.
10 ) Larsen FG, Nielsen-Kudsk F, Jakobsen P, et al: Interaction of etretinate with methotrexate pharmacokinetics in psoriatic patients. J Clin Pharmacol 1990; 30:802-807.
Bexarotene Overview
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Bexarotene is used to treat cutaneous T-cell lymphoma (CTCL, a type of skin cancer) in people whose disease could not be treated successfully with at least one other medication. Bexarotene is in a class of medications called retinoids. It works by stopping the growth of cancer cells.
Methotrexate Overview
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Methotrexate is used to treat severe psoriasis (a skin disease in which red, scaly patches form on some areas of the body) that cannot be controlled by other treatments. Methotrexate is also used along with rest, physical therapy, and sometimes other medications to treat severe active rheumatoid arthritis (RA; a condition in which the body attacks its own joints, causing pain, swelling, and loss of function) that cannot be controlled by certain other medications. Methotrexate is also used to treat certain types of cancer including cancers that begin in the tissues that form around a fertilized egg in the uterus, breast cancer, lung cancer, certain cancers of the head and neck, certain types of lymphoma, and leukemia (cancer that begins in the white blood cells). Methotrexate is in a class of medications called antimetabolites. Methotrexate treats cancer by slowing the growth of cancer cells. Methotrexate treats psoriasis by slowing the growth of skin cells to stop scales from forming. Methotrexate may treat rheumatoid arthritis by decreasing the activity of the immune system.
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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.