Colesevelam with Metformin Interaction Details

Brand Names Associated with Colesevelam

Brand Names Associated with Metformin

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

Interaction Effect

Increased exposure to extended-release metformin

Interaction Summary

The administration of colesevelam 3.75 g with metformin extended-release 1500 mg increased AUC (0 to infinity) by 44% and Cmax by 8%, in an in vivo drug-interaction study. If concurrent therapy is required, monitor the patients' glycemic control[1].

Severity

Moderate

Onset

Unspecified

Evidence

Probable

How To Manage Interaction

Colesevelam may increase exposure to extended-release metformin. If concurrent therapy with colesevelam and extended-release metformin is necessary, monitor the patients' glycemic control[1].

Mechanism Of Interaction

Unknown

References

1 ) Product Information: WELCHOL oral tablets, oral suspension, colesevelam HCl oral tablets, oral suspension. Daiichi Sankyo Inc (per FDA), Basking Ridge, NJ, 2020.

Colesevelam Overview

• Colesevelam is used in adults along with diet, weight loss, and exercise to reduce the amount of cholesterol and certain fatty substances in the blood alone or in combination with other cholesterol-lowering medications known as HMG-CoA reductase inhibitors (statins). Colesevelam is also used alone or in combination with HMG-CoA reductase inhibitors in certain boys and in girls, ages 10 to 17, with familial heterozygous hypercholesterolemia (an inherited condition in which cholesterol cannot be removed from the body normally) to decrease the amount of cholesterol and other fatty substances in the blood. Colesevelam is also used along with diet and exercise to control blood sugar levels in adults with type 2 diabetes (condition in which the body does not use insulin normally and therefore cannot control the amount of sugar in the blood). Colesevelam is in a class of medications called bile acid sequestrants. It works by binding bile acids in your intestines to form a product that is removed from the body.

• Bile acids are made when cholesterol is broken down in your body. Removing these bile acids helps to lower your blood cholesterol. 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.

Metformin Overview

• Metformin is used alone or with other medications, including insulin, to treat type 2 diabetes (condition in which the body does not use insulin normally and, therefore, cannot control the amount of sugar in the blood). Metformin is in a class of drugs called biguanides. Metformin helps to control the amount of glucose (sugar) in your blood. It decreases the amount of glucose you absorb from your food and the amount of glucose made by your liver. Metformin also increases your body's response to insulin, a natural substance that controls the amount of glucose in the blood. Metformin is not used to treat type 1 diabetes (condition in which the body does not produce insulin and therefore cannot control the amount of sugar in the blood).

• Over time, people who have diabetes and high blood sugar can develop serious or life-threatening complications, including heart disease, stroke, kidney problems, nerve damage, and eye problems. Taking medication(s), making lifestyle changes (e.g., diet, exercise, quitting smoking), and regularly checking your blood sugar may help to manage your diabetes and improve your health. This therapy may also decrease your chances of having a heart attack, stroke, or other diabetes-related complications such as kidney failure, nerve damage (numb, cold legs or feet; decreased sexual ability in men and women), eye problems, including changes or loss of vision, or gum disease. Your doctor and other healthcare providers will talk to you about the best way to manage your diabetes.

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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.