The Sound of Evolution
Colesevelam
Mechanism of action:
Colesevelam is a bile acid sequestrant resin. Colesevelam 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. Levy P et al. (2010). The potential role of colesevelam in the management of prediabetes and type 2 diabetes mellitus. Postgrad Med.
2. Staels B et al. (2009). A review of bile acid sequestrants: potential mechanism(s) for glucose-lowering effects in type 2 diabetes mellitus. Postgrad Med.