Bile Acid Sequestrants: Do They Have a Future?

  • S. M. Grundy
Part of the Proceedings in Life Sciences book series (LIFE SCIENCES)


It has been known for many years that interruption of the enterohepatic circulation (EHC) of bile acids will lower the plasma cholesterol. Interruption of the EHC can be achieved in several ways, but the usual means is by use of resins (sequestrants) that bind bile acids in the intestine and prevent their reabsorption. The bile acid sequestrants most commonly used are cholestyramine and colestipol. Cholestyramine was the drug used in the Lipid Research Clinics (LRC) Coronary Primary Prevention Trial (CPPT) (1,2). This trial tested cholestyramine vs placebo in about 4000 men with hypercholesterolemia who were treated for 7 years. Cholestyramine produced a significant lowering of the plasma cholesterol, and rates of coronary heart disease (CHD) were reduced significantly at p<0.05. This trial has generally been accepted as strong support for the “lipid hypothesis”, namely, that a lowering of the plasma cholesterol will decrease the risk for CHD. Furthermore, analysis of the trial results provided no consistent evidence that lowering of plasma cholesterol by bile acid sequestrants is accompanied by significant side effects. On the other hand, despite the success of the CPPT, doubts remain whether bile acid sequestrants have a significant future for the treatment of hypercholesterolemia. They are bulky and inconvenient to take. They can cause gastrointestinal distress, and they almost uniformly cause constipation. Also, they are only moderately effective for lowering of plasma cholesterol; and finally they are expensive.


Bile Acid Reductase Inhibitor Plasma Cholesterol Bile Acid Sequestrant Lipid Research Clinic 
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Copyright information

© Springer-Verlag Berlin Heidelberg 1987

Authors and Affiliations

  • S. M. Grundy
    • 1
  1. 1.Center for Human Nutrition, Department of Clinical NutritionUniversity of Texas Health Science Center at DallasDallasUSA

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