Cholestyramine with Mycophenolate Mofetil Interaction Details

Brand Names Associated with Cholestyramine

Brand Names Associated with Mycophenolate Mofetil

Medical Content Editor Dr. Brian Staiger, PharmD
Last updated Feb 28, 2024

Interaction Effect

Reduced exposure to mycophenolic acid (MPA), the active metabolite of mycophenolate mofetil

Interaction Summary

Exposure to mycophenolate mofetil may be reduced with concomitant administration of a bile acid sequestrant (BAS). The AUC of mycophenolic acid (MPA), the active metabolite of mycophenolate mofetil, was decreased by about 40% with a single dose of mycophenolate mofetil 1.5 g after being pretreated with cholestyramine 4 g 3 times daily for 4 days. This decrease was consistent with interruption of enterohepatic recirculation, possibly due to intestinal binding by cholestyramine of recirculating MPAG (an inactive metabolite that is reconverted to MPA). Monitor patients for alterations in efficacy or mycophenolate mofetil-related adverse effects when these drugs are coadministered. Obtaining MPA plasma levels before and after the initiation or discontinuation of concomitant medications may be necessary to ensure MPA levels remain stable[1].

Severity

Major

Onset

Rapid

Evidence

Theoretical

How To Manage Interaction

Exposure to mycophenolate mofetil may be reduced with concomitant administration of a bile acid sequestrant (BAS) due to binding of recirculating MPAG (metabolite of mycophenolate mofetil) by the BAS resulting in interference with enterohepatic recirculation of mycophenolic acid (MPA). Monitor patients for alterations in efficacy or mycophenolate mofetil-related adverse effects when these drugs are coadministered. Obtaining MPA plasma levels before and after the initiation or discontinuation of concomitant medications may be necessary to ensure MPA levels remain stable[1].

Mechanism Of Interaction

Colestipol interruption of enterohepatic recirculation of mycophenolic acid

Literature Reports

A) The AUC of mycophenolic acid (MPA) was decreased by about 40% during a study in 12 healthy volunteers who received a single dose of mycophenolate mofetil 1.5 g after being pretreated with cholestyramine 4 g 3 times daily for 4 days [1].

References

1 ) Product Information: CELLCEPT(R) oral capsules, oral tablets, oral suspension, intravenous injection, mycophenolate mofetil oral capsules, oral tablets, oral suspension, intravenous injection. Genentech USA, Inc (per FDA), South San Francisco, CA, 2019.

Cholestyramine Overview

• Cholestyramine is used with diet changes (restriction of cholesterol and fat intake) to reduce the amount of cholesterol and certain fatty substances in your blood. 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 to prevent heart disease, angina (chest pain), strokes, and heart attacks.

• This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.

Mycophenolate Mofetil Overview

• Mycophenolate (CellCept) is used with other medications to help prevent transplant organ rejection (attack of the transplanted organ by the immune system of the person receiving the organ) in adults and children 3 months of age and older who have received kidney, heart, or liver transplants. Mycophenolate (Myfortic) is used with other medications to help prevent the body from rejecting kidney transplants in adults and children 5 years of age and older. Mycophenolate is in a class of medications called immunosuppressive agents. It works by weakening the body's immune system so it will not attack and reject the transplanted organ.

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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:

• Gold Standard Drug Database
• Micromedex
• Lexicomp
• DrugBank

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.