Bile Acid Sequestrants

What are some examples of bile acid sequestrants available in the U.S.?

Examples include:

• cholestyramine (Questran, Questran Light, Prevalite, LoCholest),
  
  
• colestipol (Colestid), and
  
  
• colesevelam (WelChol).

How do bile acid sequestrants work?

These drugs bind with cholesterol-containing bile acids in the intestines and are then eliminated in the stool. The usual effect of bile acid sequestrants is to lower LDL cholesterol by about 10%-20%. Small doses of sequestrants can produce useful reductions in LDL cholesterol. Bile acid sequestrants are sometimes prescribed in combination with a statin to enhance cholesterol reduction. When these drugs are combined, their effects are added together to lower LDL cholesterol by more than 40%. These drugs are not effective for lowering triglycerides.

Who should not use these bile acid sequestrants?

Individuals who are allergic to bile acid sequestrants or who have a medical history of bile obstruction should not use these agents. Patients with phenylketonuria should not take aspartame-containing bile acid sequestrants such as Questran Light.

Use: Bile acid sequestrant powders must be mixed with water or fruit juice and are typically taken once or twice (rarely, three times) daily with meals. Tablets must be taken with large amounts of fluids to avoid stomach and intestinal problems.

Drug or food interactions: Bile acid sequestrants decrease the ability of the body to absorb numerous drugs such as:

• warfarin (Coumadin),
• thyroid hormone,
  
  
• amiodarone,
  
  
• sulindac (Clinoril),
  
  
• methotrexate (Rheumatrex, Trexall),
  
  
• digoxin (Lanoxin),
  
  
• glipizide (Glucotrol),
  
  
• phenytoin (Dilantin),
  
  
• imipramine (Tofranil),
  
  
• niacin (Niacor, Niaspan, Slo-Niacin),
  
  
• methyldopa,
  
  
• tetracycline (Sumycin),
  
  
• clofibrate (Atromid-S),
  
  
• hydrocortisone,
  
  
• ezetimibe (Zetia), or
  
  
• penicillin.

They also inhibit the absorption of fat-soluble vitamins (including vitamin A and E); thus, patients taking these agents for a long time may need vitamin supplementation. Take bile acid sequestrants two hours before or after antacids, since antacids may decrease their effectiveness. Talk to your doctor or pharmacist for more information about the best time to take your medications.

Side effects: Bile acid sequestrants are not absorbed from the gastrointestinal tract, and 30 years of experience with these drugs indicates that long-term use is safe. These agents may cause constipation, bloating, nausea, or gas.

Viewer Comments & Reviews

Cholesterol Lower Medications - Your Experience

The eMedicineHealth physician editors ask:

Please describe your experience with cholesterol lowering medications.

Anonymously share your comment to help others.
See 2 Viewer Comments & Reviews

Submit Your Review