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Multiple Choice

Cholestyramine belongs to which class of lipid-lowering agents?

Cholestyramine is a bile-acid sequestrant. It works by binding bile acids in the intestine, preventing their reabsorption. This reduces the bile acid pool, prompting the liver to convert more cholesterol into bile acids and to upregulate LDL receptors on liver cells. The result is more clearance of LDL cholesterol from the blood, giving a meaningful drop in LDL-C levels. This mechanism is different from statins, which inhibit cholesterol synthesis in the liver; fibrates, which mainly lower triglycerides and raise HDL via PPAR-alpha activation; and PCSK9 inhibitors, which are antibodies that prevent LDL receptor degradation to increase LDL receptor availability. Cholestyramine’s action—binding bile acids to interrupt their reabsorption—explains why it’s categorized as a bile-acid sequestrant.

Cholestyramine is a bile-acid sequestrant. It works by binding bile acids in the intestine, preventing their reabsorption. This reduces the bile acid pool, prompting the liver to convert more cholesterol into bile acids and to upregulate LDL receptors on liver cells. The result is more clearance of LDL cholesterol from the blood, giving a meaningful drop in LDL-C levels.

This mechanism is different from statins, which inhibit cholesterol synthesis in the liver; fibrates, which mainly lower triglycerides and raise HDL via PPAR-alpha activation; and PCSK9 inhibitors, which are antibodies that prevent LDL receptor degradation to increase LDL receptor availability. Cholestyramine’s action—binding bile acids to interrupt their reabsorption—explains why it’s categorized as a bile-acid sequestrant.