1. Cholesterol Levels Slideshow Pictures
2. Lower Cholesterol Slideshow: Avoid Heart Disease
3. Take the Cholesterol Quiz

Medical Author:

Omudhome Ogbru, PharmD

Omudhome Ogbru, PharmD

Dr. Ogbru received his Doctorate in Pharmacy from the University of the Pacific School of Pharmacy in 1995. He completed a Pharmacy Practice Residency at the University of Arizona/University Medical Center in 1996. He was a Professor of Pharmacy Practice and a Regional Clerkship Coordinator for the University of the Pacific School of Pharmacy from 1996-99.

View Full Profile

Medical Editor:

Melissa Conrad Stöppler, MD, Chief Medical Editor

Melissa Conrad Stöppler, MD, Chief Medical Editor

Melissa Conrad Stöppler, MD, is a U.S. board-certified Anatomic Pathologist with subspecialty training in the fields of Experimental and Molecular Pathology. Dr. Stöppler's educational background includes a BA with Highest Distinction from the University of Virginia and an MD from the University of North Carolina. She completed residency training in Anatomic Pathology at Georgetown University followed by subspecialty fellowship training in molecular diagnostics and experimental pathology.

View Full Profile

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.

Must Read Articles Related to Understanding Cholesterol-Lowering Medications

Cholesterol FAQs Test your cholesterol IQ by reading about cholesterol FAQs (cholesterol facts) like the risk factors for high cholesterol (diet, lack of exercise, smoking, here...learn more >>

Lifestyle Cholesterol Management Lifestyle cholesterol management is important to lower your risk for heart disease (heart attack, stroke, and peripheral artery disease). Cholesterol management...learn more >>

Statins and Cholesterol Statins are a class of drug prescribed for reducing blood cholesterol levels in individuals with high cholesterol. Examples of statins available include: atorva...learn more >>

See the Entire Understanding Cholesterol-Lowering Medications Topic Guide »