Medications and Drugs
Bile Acid Sequestrants
Medical Author : Dennis Lee, M.D.
Medical Editor:
Daniel Kulick, M.D.
What are bile acid sequestrants?
Bile acid sequestrants such as cholestyramine (Questran), colestipol
(Colestid), and colesevelam (Welchol) are medications for lowering LDL
cholesterol. Bile acid sequestrants bind bile acids in the intestine and cause
more of the bile acids to be excreted in the stool. This reduces the amount of
bile acids returning to the liver and forces the liver to produce more bile
acids to replace the bile acids lost in the stool. In order to produce more bile
acids, the liver converts more cholesterol into bile acids, which lowers the
level of cholesterol in the blood.
Bile acid sequestrants have modest LDL cholesterol lowering effects. Low
doses (for example 8 gram/day of Cholestyramine) can lower LDL cholesterol by
10%-15 %. But even high doses (24 gram/day of cholestyramine) can only lower LDL
cholesterol by approximately 25%. Therefore, bile acid sequestrants used alone
are not as effective as statins in lowering LDL cholesterol.
However, bile acid sequestrants are most useful in combining with a statin or
niacin to aggressively lower LDL cholesterol levels. The statin-bile acid
sequestrant combination can lower LDL cholesterol levels by approximately 50%,
lower than a statin alone. A statin-niacin combination can substantially reduce
LDL cholesterol and elevate HDL cholesterol.
What are the side effects of bile acid sequestrants?
Bile acid sequestrants are not absorbed into the body and therefore they do
not have systemic side effects (affecting other organs). Therefore, their most
common side effects are gastrointestinal;
Bile acid sequestrants can bind to and decrease the absorption (and hence the
effectiveness) of other drugs, such as warfarin (Coumadin), thyroid hormones
(Synthroid, Levoxyl), digoxin (Lanoxin), thiazide diuretics (Hydrodiuril,
Oretic, Dyazide, Maxzide), and many others. Therefore, these medications should
be taken 1 hour before or 4-6 hours after the administration of a bile acid
sequestrant.
Bile acid sequestrants reduces the absorption of vitamin A, D, E, and K.
Long-term use may thus cause a deficiency of vitamin A, D, E, and K.
Reference: FDA Prescribing Information
Last Editorial Review: 4/5/2005
Report Problems to the Food and Drug Administration
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit the FDA MedWatch website or call 1-800-FDA-1088.
- cholestyramine, Questran - Explains the medication cholestyramine (Questran), a drug used for reducing cholesterol levels in the blood, to relieve the itching of liver and biliary disease, and to treat overdoses of digoxin or thyroid hormone.
- Diarrhea - Read the causes of diarrhea including infections, parasites, food poisoning, medications, IBS, IBD, cancer, endocrine disease, fat malabsorption, laxative abuse and more.
- colestipol, Colestid - Information about colestipol (Colestid), an oral cholesterol lowering medication. Colestid is also prescribed for the treatment of diarrhea due to increased intestinal bile, and itching associated with liver disease.
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