Bile acid sequestrant (intestinal)

Bile acid sequestration in the intestine is a pharmacologic action where synthetic polymeric anion-exchange resins bind to bile acids in the gut, preventing their reabsorption into the enterohepatic circulation[1][3][5]. This leads to increased hepatic conversion of cholesterol to bile acids and upregulation of hepatic LDL receptors, thereby lowering serum LDL cholesterol. Clinically, bile acid sequestrants are used in the management of hypercholesterolemia, chronic diarrhea due to bile acid malabsorption, and as an adjunct in type 2 diabetes. These compounds are not proteins, receptors, enzymes, or genes, but synthetic, insoluble, and non-absorbed polymers that act locally within the gastrointestinal tract. The most widely used drugs in this category are cholestyramine, colestipol, and colesevelam. While generally safe, their main side effects are gastrointestinal, and caution is needed regarding fat-soluble vitamin absorption and possible interactions with other oral medications[1][5][7].

Other names

Bile acid resinantilipemic agent (bile acid sequestrant)cholesterol-lowering resin

Binds and sequesters bile acids in intestine, preventing reabsorption; this depletes bile acid pool, increases hepatic cholesterol conversion to bile acids, and upregulates LDL receptor expression, lowering serum LDL-C