Gosset Molecular Classification
Anion exchange resin, Polymeric drug
Other Names
Bile acid resins, Cholestyramine, Colestipol, Colesevelam
Disease Roles
Bile Acid Sequestrant Overview
Bile acid sequestrants are non-absorbable polymeric resins that bind to bile acids in the gastrointestinal tract, preventing their reabsorption and promoting their excretion. This leads to a reduction in LDL cholesterol levels. They are used in the treatment of hypercholesterolemia, bile acid malabsorption, and pruritus associated with cholestasis. Common examples include cholestyramine, colestipol, and colesevelam.
Mechanism of Action
Binds bile acids in the gastrointestinal tract, preventing their reabsorption and promoting their excretion in feces. This forces the liver to convert more cholesterol into bile acids, lowering LDL cholesterol levels.
Biological Functions
Bile acid binding
Cholesterol reduction
Fecal excretion of bile acids
Disease Associations
Hypercholesterolemia
Bile acid malabsorption
Pruritus related to cholestasis
Type 2 diabetes mellitus
Safety Considerations
- Constipation
- Bloating
- Abdominal pain/discomfort
- Flatulence
- Nausea/vomiting
- Diarrhea
- Gallstone formation
- Reduced absorption of other medications
- Vitamin deficiencies (A, D, E, K)
Interacting Drugs
Cholestyramine
Colestipol
Colesevelam
Statins
Fat-soluble vitamins (A, D, E, K)
Other orally administered drugs (potential for reduced absorption)