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Multiple Choice

Cholestyramine's mechanism of action involves which of the following?

Cholestyramine lowers LDL cholesterol by binding bile acids in the gut. By sequestering bile acids in the intestinal lumen, it prevents their reabsorption and disrupts the enterohepatic circulation. In response, the liver uses more cholesterol to synthesize new bile acids, which reduces hepatic cholesterol stores and triggers upregulation of LDL receptors. This increases the clearance of LDL from the bloodstream, resulting in lower LDL-C. This mechanism is different from inhibiting HMG-CoA reductase (as statins do), which reduces cholesterol synthesis; from inhibiting dietary fat absorption (as with orlistat); or from activating lipoprotein lipase (a mechanism more associated with certain fibrates).

Cholestyramine lowers LDL cholesterol by binding bile acids in the gut. By sequestering bile acids in the intestinal lumen, it prevents their reabsorption and disrupts the enterohepatic circulation. In response, the liver uses more cholesterol to synthesize new bile acids, which reduces hepatic cholesterol stores and triggers upregulation of LDL receptors. This increases the clearance of LDL from the bloodstream, resulting in lower LDL-C.

This mechanism is different from inhibiting HMG-CoA reductase (as statins do), which reduces cholesterol synthesis; from inhibiting dietary fat absorption (as with orlistat); or from activating lipoprotein lipase (a mechanism more associated with certain fibrates).