Ezetimibe Ezetimibe is a new type of selective cholesterol absorption inhibitor that inhibits the absorption of cholesterol in the small intestine and through bile transport to the gut, reducing cholesterol levels in the serum and liver by combining with membrane proteins (relative molecular weight 145 X 103) in the small intestine brush-like membrane vesicles. Unlike cholic acid chelating agents, ezetimibe ezetimibe does not affect the absorption of cholesterol esters, other steroids (such as bezoar bile acid), triglyceride and fat-soluble vitamins. Its pharmacological action has nothing to do with the inhibition of acetyl coenzyme A-cholesterol acetyl transferase (ACAT) and the expression of the LDL receptor (scavenger receptor). Ezetimibe Ezetimibe was absorbed in the liver after the combination of glucose and glyoxylic acid through the intestinal cycle, almost specific location in the small intestine mucosa cells.
The rat radioisotope experiment confirmed that ezetimibe Ezetimibe had no direct effect on the synthesis of cholesterol in the small intestine and liver, only by preventing exogenous cholesterol in the intestinal tract vesicles (Enterocyte) from being transported to intracellular cholesterol pools (Cholesterol pool), inhibiting exogenous cholesterol transport to lymph, but without affecting the newly synthesized cholesterol (endogenous) synthesis into the small intestine lipoprotein. Ezetimibe Ezetimibe also inhibits the uptake of plant sterols and becomes the first therapeutic drug to treat rare inherited plant-sterol blood.