Bile acid sequestrants

What are Bile acid sequestrants?

Bile acid sequestrants are used to reduce low density lipoprotein (LDL) cholesterol levels. After oral administration, they are not absorbed but bind to bile acids (which contains cholesterol) in the intestine and prevent their reabsorption into the body. The bound complex is insoluble and is excreted in the faeces. Decrease in bile acid leads to an increase in hepatic synthesis of bile acids from cholesterol. Depletion of cholesterol increases LDL receptor activity, therefore increases removal of LDL cholesterol from the blood.

Bile acid sequestrants, including colesevelam, colestipol, and cholestyramine, are approved by the Food and Drug Administration (FDA) in combination with restriction of dietary saturated and trans-fatty acids to manage hypercholesterolemia.

Three commonly used bile acid sequestrants are cholestyramine, colestipol, and the newer agent colesevelam (Table 23-5). Both cholestyramine and colestipol are packaged as powders and need to be mixed with liquid before consumption.

Statins are the most potent drugs for lowering LDL-C and are well tolerated in most patients. The addition of a bile acid sequestrant or ezetimibe to a statin produces additional LDL-C reduction allowing many patients to reach LDL-C targets.