Bile Acid Sequestrants

  • Pharmacy Author:
    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.

  • Medical and Pharmacy Editor: Jay W. Marks, MD
    Jay W. Marks, MD

    Jay W. Marks, MD

    Jay W. Marks, MD, is a board-certified internist and gastroenterologist. He graduated from Yale University School of Medicine and trained in internal medicine and gastroenterology at UCLA/Cedars-Sinai Medical Center in Los Angeles.

What are bile acid sequestrants?

Bile acid sequestrants such as cholestyramine (Questran, Prevalite), colestipol (Colestid, Flavored Colestid ), and colesevelam (Welchol) are medications for lowering LDL cholesterol in conjunction with diet modification.

How do bile acid sequestrants work?

Bile acid sequestrants bind bile acids in the intestine and increase the excretion of bile acids 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.

Bile acid sequestrants are most useful in combination with a statin or niacin to aggressively lower LDL cholesterol levels. The combination of a statin and bile acid sequestrant can lower LDL cholesterol levels by approximately 50%. The combination of a statin and niacin can substantially reduce LDL cholesterol and elevate HDL cholesterol.

Medically Reviewed by a Doctor on 9/28/2015

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