Cholestyramine with Aceclofenac Interaction Details

Brand Names Associated with Cholestyramine

  • Cholestyramine Resin
  • Locholest®
  • Locholest® Light
  • Prevalite®
  • Questran®
  • Questran® Light

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Last updated Feb 28, 2024

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Interaction Effect

Decreased diclofenac bioavailability

Interaction Summary

Single doses of colestipol 10 g, cholestyramine 8 g, or placebo were administered following a dose of diclofenac 100 mg to healthy volunteers in a randomized, crossover study that consisted of three phases. Results showed that the area under the concentration-time curve (AUC) of diclofenac was decreased by 33% and 62% in the presence of colestipol and cholestyramine, respectively. Maximum concentration (Cmax) was also reduced by colestipol (58%) and cholestyramine (75%)[1].

Severity

Moderate

Onset

Rapid

Evidence

Probable

How To Manage Interaction

Space the administration of cholestyramine and diclofenac as far apart as possible and monitor the patient for diclofenac efficacy.

Mechanism Of Interaction

Decreased diclofenac absorption in the gastrointestinal tract

Literature Reports

A) Six healthy male volunteers participated in a randomized crossover study which consisted of three phases to determine the effect of the bile resins colestipol and cholestyramine on the pharmacokinetics of diclofenac. Each subject ingested a single dose of diclofenac 100 mg on three occasions, followed by either cholestyramine 8 g, colestipol 10 g, or water. These doses of colestipol and cholestyramine were chosen because they are standard doses used in the treatment of hypercholesterolemia. Cholestyramine decreased the mean area under the concentration-time curve (AUC) of diclofenac by 62% (4196.5 ng/h/mL vs. 1605.2 ng/h/mL). Maximum concentration (Cmax) of diclofenac was also decreased from 3355.3 ng/mL to 838.5 ng/mL, representing a 75% reduction. Because approximately 30% to 35% of a diclofenac dose undergoes enterohepatic cycling, separating the times of administration of diclofenac and cholestyramine may not completely eliminate the possibility of this interaction [1].

References

    1 ) Al-Balla SR, El-Sayed YM, Al-Meshal MA, et al: The effects of cholestyramine and colestipol on the absorption of diclofenac in man. Int J Clin Pharmacol Ther 1994; 32:441-445.

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.

See More information Regarding Cholestyramine Resin

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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.