Cholestyramine

Cholestyramine is a bile acid sequestrant used to lower LDL cholesterol by binding bile acids in the intestine.

Structure of Cholestyramine

  • Cholestyramine is a bile acid sequestrant composed of a cross-linked polymer of divinylbenzene and polyethylene oxide, functionalized with quaternary ammonium groups.
  • Chemical Formula: (C₁₂H₁₅NO)n·Cl⁻

Structure of Cholestyramine

Mode of Action

  • Bile Acid Sequestration: Binds bile acids in the intestine, preventing their reabsorption.
  • Cholesterol Reduction: Forces the liver to convert more cholesterol into bile acids, thereby lowering blood cholesterol levels.
  • LDL-C Lowering: Reduces low-density lipoprotein cholesterol (LDL-C) by decreasing hepatic cholesterol synthesis.
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Uses

  • Hypercholesterolemia: Lowers LDL-C and total cholesterol levels.
  • Pruritus Associated with Cholestasis: Alleviates itching by binding bile acids.
  • Bile Acid Diarrhea: Manages chronic diarrhea caused by bile acid malabsorption.
  • Fibromyalgia: Sometimes used off-label for pain management.

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