Colestyramine (Cholestyramine resin)

Colestyramine (Cholestyramine) is a bile acid binding resin and can inhibit intestinal bile acid absorption which results in the increasing bile acid synthesis from cholesterol.

Colestyramine (Cholestyramine) is a bile acid binding resin and can inhibit intestinal bile acid absorption which results in the increasing bile acid synthesis from cholesterol[1]. Results reveal that GSPE treatment alone, and co-administration with Colestyramine (CHY), regulate BA, cholesterol and TG metabolism differently compare to Colestyramine (CHY) administration alone. Notably, GSPE decreases intestinal apical sodium-dependent bile acid transporter (Asbt) gene expression, while Colestyramine (CHY) significantly induces expression. Administration with GSPE or Colestyramine (CHY) robustly induces hepatic BA biosynthetic gene expression, especially cholesterol 7α-hydroxylase (Cyp7a1), compare to control, while co-administration further enhances expression. Treatment with Colestyramine (CHY) induces both intestinal and hepatic cholesterologenic gene expression, while co-administration with GSPE attenuates the Colestyramine (CHY)-inducing increase in the liver but not in the intestine. Colestyramine (CHY) also induces hepatic lipogenic gene expression, which is attenuated by co-administration with GSPE[2].

[1]. Maugeais C, et al. rHDL administration increases reverse cholesterol transport in mice, but is not additive on top of ezetimibe or cholestyramine treatment. Atherosclerosis. 2013 Jul;229(1):94-101. [2]. Rebecca M. Heidker, et al. Grape Seed Procyanidins and Cholestyramine Differentially Alter Bile Acid and Cholesterol Homeostatic Gene Expression in Mouse Intestine and Liver. PLoS One. 2016; 11(4): e0154305.