Bile acid sequestrants for high cholesterol


Generic Name Brand Name
cholestyramine Questran
colesevelam Welchol
colestipol hydrochloride Colestid

Sequestrants are sometimes called bile acid resins or gels.

How It Works

Sequestrants bind to bile acids in the intestine and prevent them from being reabsorbed into the blood. The liver then produces more bile to replace the bile that has been lost. Because the body needs cholesterol to make bile, the liver uses up the cholesterol in the blood, which reduces the amount of LDL cholesterol circulating in the blood.

Some of these medicines are a powder that you mix with water, fruit juice, or milk (mixing them with carbonated beverages causes belching). The powder can also be mixed with foods such as applesauce, soup, canned pears, or peaches.

Some of these medicines come in tablet form.

Why It Is Used

Low doses of these medicines may be prescribed, along with dietary therapy, to lower LDL cholesterol in people who have high cholesterol and known heart disease or in people who are at high risk for heart disease.

For people who have very high cholesterol levels (over 240 mg/dL or 6.21 mmol/L), these drugs also may be prescribed in combination with medicines called statins.

People who have the following conditions should not take sequestrants:

  • High triglycerides (more than 200 mg/dL)
  • Familial dysbetalipoproteinemia (a rare form of lipid disorder)
  • Severe constipation (sequestrants make constipation worse)

How Well It Works

Bile acid sequestrants:

  • Reduce LDL cholesterol by 15% to 30%.1
  • Raise HDL cholesterol by 3% to 5%.1
  • May increase triglycerides, so you should not take these medicines if your triglyceride levels are above 300 mg/dL.1

Side Effects

Bile acid sequestrants are considered safe for long-term use.

  • The most common side effects are constipation, bloating, fullness, nausea, and gas.
  • Starting with a single daily dose and gradually adding doses as needed is a good way to find the dose level that minimizes these common side effects. Mixing the powdered forms of these drugs with fiber laxatives (such as Citrucel or Metamucil) may help constipation problems. Some doctors believe combining Metamucil with bile acid sequestrants may help lower LDL cholesterol.

See Drug Reference for a full list of side effects. (Drug Reference is not available in all systems.)

What To Think About

Bile acid sequestrants may interfere with the absorption of other drugs and vitamins. Tell your doctor what other medicines you take, including nonprescription medicines.

Other medicines should be taken 1 hour before or 4 hours after sequestrants. But bile acid sequestrants may be beneficial when combined with statins. If you need to take antibiotics for an infection, ask your doctor whether you should stop taking the bile acid sequestrant until you have finished the course of antibiotics.

Some people do not like the taste or texture of the sequestrants. Mixing the medicine in foods like applesauce, soup, canned pears, or peaches, instead of mixing it in a beverage, may help.

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  1. Grundy SM, et al. (2001). Executive summary of the third report of the National Cholesterol Education Program (NCEP) Expert Panel on Detection, Evaluation, and Treatment of High Blood Cholesterol in Adults (Adult Treatment Panel III). JAMA, 285(19): 2486–2497.

Last Updated: July 11, 2008

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