Molecular Classification
Physicochemical Interaction, Sequestration, Ion-exchange resin
Other Names
Bile Acid Binding, Bile Acid Adsorption, Bile Acid Exchange
Disease Roles
HypercholesterolemiaBile Acid MalabsorptionPruritus associated with cholestasis

Bile Acid Sequestration Overview

Bile acid sequestration is a process by which bile acid sequestrants bind bile acids in the gastrointestinal tract, preventing their reabsorption and leading to increased fecal excretion. This interrupts enterohepatic circulation, forcing the liver to convert more cholesterol into bile acids, ultimately reducing circulating LDL cholesterol levels. While it's a process, it's targeted therapeutically to manage various conditions.

Mechanism of Action

Binds bile acids in the gastrointestinal tract, preventing their reabsorption and promoting their excretion in feces. This leads to increased hepatic conversion of cholesterol into bile acids, lowering serum LDL cholesterol.

Biological Functions

Lipid metabolism regulation
Cholesterol homeostasis
Bile acid homeostasis
Enterohepatic circulation disruption

Disease Associations

Hypercholesterolemia
Bile Acid Malabsorption
Pruritus associated with cholestasis
Type 2 Diabetes (adjunctive therapy)

Safety Considerations

  • Gastrointestinal side effects (constipation, bloating, abdominal pain, flatulence, diarrhea)
  • Drug interactions (reduced absorption of other medications)
  • Potential for increased triglycerides

Interacting Drugs

Cholestyramine
Colestipol
Colesevelam