Cholestyramine with Cerivastatin Interaction Details
Brand Names Associated with Cholestyramine
- Cholestyramine Resin
- Locholest®
- Locholest® Light
- Prevalite®
- Questran®
- Questran® Light
Medical Content Editor Dr. Brian Staiger, PharmD
Last updated
Feb 28, 2024
Interaction Effect
Reduced cerivastatin absorption and clinical efficacy
Interaction Summary
In healthy subjects, cerivastatin area under the concentration-time curve (AUC) was decreased by 22% and the peak cerivastatin serum level was decreased by 40% when given concurrently with cholestyramine. This interaction can be minimized by the administration of cholestyramine one hour before the evening meal and the administration of cerivastatin four hours after the same evening meal, which results in only an 8% decrease of the cerivastatin AUC[1][2].
Severity
Moderate
Onset
Rapid
Evidence
Probable
How To Manage Interaction
Cerivastatin should be spaced 1 hour before or 4 hours after cholestyramine usage to minimize this interaction. Administration of cholestyramine before the evening meal and the administration of cerivastatin at bedtime is preferred.
Mechanism Of Interaction
Binding of cerivastatin
Literature Reports
A) Twelve healthy male volunteers received single oral doses of cerivastatin 200 mcg with 250 mL of water or with cholestyramine 12 g in a controlled, randomized, nonblind two-way crossover study. Drugs were administered under fasting conditions, and a seven-day washout interval elapsed between the study phases. The cerivastatin area under the concentration-time curve (AUC) decreased from 10.3 mcg/h/L to 8.10 mcg/h/L when cholestyramine was coadministered. Likewise, the maximum concentration (Cmax) decreased from 2.28 mcg/L to 1.33 mcg/L, and the time to maximum concentration (tmax) increased from 2.5 hours to 3.0 hours. The half-life (t1/2) also increased from 2.2 hours to 2.6 hours in the presence of cholestyramine [2].
B) In a study involving 12 healthy Caucasian males, the influence of cholestyramine pretreatment on cerivastatin pharmacokinetics was investigated. Subjects received the following treatments during this controlled, randomized, nonblind, four-way crossover study: cerivastatin 300 mcg at the beginning of dinner, cholestyramine 12 g one hour before dinner and cerivastatin 300 mcg at the beginning of dinner, cerivastatin 300 mcg four hours after dinner, and cholestyramine 12 g one hour before dinner and cerivastatin 300 mcg four hours after dinner. Cerivastatin area under the concentration-time curve (AUC) decreased 8% when administered five hours apart from cholestyramine and 16% when administered at only a one-hour interval. Maximum concentration (Cmax) decreased approximately 32%, despite of the time of cholestyramine administration [2].
References
1 ) Product Information: Baycol(R), cerivastatin sodium. Bayer Corporation, West Haven, CT, 1999.
2 ) Muck W, Ritter W, Frey R, et al: Influence of cholestyramine on the pharmacokinetics of cerivastatin. Int J Clin Pharmacol Ther 1997; 35:250-254.
Cholestyramine Overview
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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.
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This medication is sometimes prescribed for other uses; ask your doctor or pharmacist for more information.
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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.
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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.
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