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Bile acid sequestrants for cholesterol

Antilipemic agent; Bile acid resins; Colestipol (Colestid); Cholestyramine (Locholest, Prevalite, and Questran); Colesevelam (Welchol)

Bile acid sequestrants are medicines that help lower your LDL (bad) cholesterol. Too much cholesterol in your blood can stick to the walls of your arteries and narrow or block them.

These medicines work by blocking bile acid in your stomach from being absorbed in your blood. Your liver then needs the cholesterol from your blood to make more bile acid. This reduces your cholesterol level.

This medicine also may help people with type 2 diabetes manage their blood sugar.

How Bile Acid Sequestrants Help

Improving your cholesterol levels can help protect you from:

  • Heart disease
  • Heart attack
  • Stroke

Your health care provider will work with you to lower your cholesterol by improving your diet. If this is not successful, medicines to lower the cholesterol may be the next step.

Statins are thought to be the best drugs to use for people who need medicines to lower their cholesterol.

Some people may be prescribed these medicines in combination with other drugs. They may also need to take them if other medicines are not tolerated due to allergies or side effects.

Both adults and teenagers can use this medicine when needed.

How to Take Bile Acid Sequestrants

Take your medicines as directed. You may take this medicine 1 to 2 times per day or more often in smaller doses. Do not stop taking your medicine without first talking with your provider.

This medicine comes in pill or powder form.

  • You will need to mix powder forms with water or other fluids.
  • The powder may also be mixed with soups or blended fruit.
  • Pill forms should be taken with plenty of water.
  • Do not chew or crush the pill.

You should take this medicine with food, unless otherwise directed.

Store all of your medicines in a cool, dry place. Keep them where children cannot get to them.

You should follow a healthy diet while taking bile acid sequestrants. This includes eating less fat in your diet. Other ways you can help your heart include:

  • Getting regular exercise
  • Managing stress
  • Quitting smoking

Know Your Risks

Before you start taking bile acid sequestrants, tell your provider if you:

  • Have bleeding problems or stomach ulcers
  • Are pregnant, plan to become pregnant, or are breastfeeding
  • Have allergies
  • Are taking other medicines
  • Plan to have surgery or dental work

If you have certain conditions, you may need to avoid this medicine. These include:

  • Liver or gallbladder problems
  • High triglycerides
  • Heart, kidney, or thyroid conditions

Tell your provider about all of your medicines, supplements, vitamins, and herbs. Certain medicines may interact with bile acid sequestrants. Be sure to tell your provider before taking any new medicines.

Taking this medicine may also affect how vitamins and other medications are absorbed in the body. Ask your provider if you should take a multivitamin supplement.

Regular blood tests will tell you and your provider how well the medicine is working.

Side Effects

Constipation is the most common side effect. Other possible side effects may include:

  • Heartburn
  • Gas and bloating
  • Diarrhea
  • Nausea
  • Muscles aches and pains

When to Call the Doctor

You should contact your provider if you have:

  • Vomiting
  • Sudden weight loss
  • Bloody stools or bleeding from the rectum
  • Bleeding gums
  • Severe constipation

References

American Heart Association website. Cholesterol medications. www.heart.org/en/health-topics/cholesterol/prevention-and-treatment-of-high-cholesterol-hyperlipidemia/cholesterol-medications. Updated February 20, 2024. Accessed March 5, 2024.

Arnett DK, Blumenthal RS, Albert MA, et al. 2019 ACC/AHA Guideline on the primary prevention of cardiovascular disease: A report of the American College of Cardiology/American Heart Association Task Force on clinical practice guidelines. Circulation. 2019;140(11):e596-e646. PMID: 30879355 pubmed.ncbi.nlm.nih.gov/30879355/.

Genest J, Mora S, Libby P. Lipoprotein disorders and cardiovascular disease. In: Libby P, Bonow RO, Mann DL, Tomaselli GF, Bhatt DL, Solomon SD, eds. Braunwald's Heart Disease: A Textbook of Cardiovascular Medicine. 12th ed. Philadelphia, PA: Elsevier; 2022:chap 27.

Grundy SM, Stone NJ, Bailey AL, et al. 2018 AHA/ACC/AACVPR/AAPA/ABC/ACPM/ ADA/AGS/APhA/ASPC/NLA/PCNA guideline on the management of blood cholesterol: a report of the American College of Cardiology/American Heart Association Task Force on Clinical Practice Guidelines. J Am Coll Cardiol. 2019;73(24):3234-3237. PMID: 30423391 pubmed.ncbi.nlm.nih.gov/30423391/.

Nambi V, Ballantyne CM, Jones PH. Overview of general approach to management of dyslipidemias. In: Ballantyne CM, ed. Clinical Lipidology: A Companion to Braunwald's Heart Disease. 3rd ed. Philadelphia, PA: Elsevier; 2024:chap 11.

Norata GD, Catapano AL. Cholesterol absorption inhibitors. In: Ballantyne CM, ed. Clinical Lipidology: A Companion to Braunwald's Heart Disease. 3rd ed. Philadelphia, PA: Elsevier ; 2024:chap 18.

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Review Date: 2/27/2024

Reviewed By: Thomas S. Metkus, MD, Assistant Professor of Medicine and Surgery, Johns Hopkins University School of Medicine, Baltimore, MD. Also reviewed by David C. Dugdale, MD, Medical Director, Brenda Conaway, Editorial Director, and the A.D.A.M. Editorial team.

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