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Colestipol


Mechanism of action:

Colestipol is a bile acid sequestrant resin. Colestipol is not absorbed in the intestine. Instead, it forms nonabsorbable complexes with bile acids, preventing their reabsorption in the ileum and causing them to be excreted in the feces. As a result, bile acid excretion increases and hepatic bile acid levels decrease. To synthesize new bile acids, hepatocytes increase the expression of the low-density lipoprotein (LDL) receptor, thereby enhancing the uptake and breakdown of LDL from the bloodstream. Ultimately, this lowers the plasma concentration of low-density lipoprotein cholesterol (LDL-C).

Reference(s):

1. LaRosa JC et al. (1982). The mechanism of action of lipid-lowering drugs. Angiology. 


2. Farmer JA et al. (1995). Currently available hypolipidaemic drugs and future therapeutic developments. Baillieres Clin Endocrinol Metab.

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