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 145x103) 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 confirms that ezetimibe ezetimibe has no direct effect on the synthesis of cholesterol in the small intestine and liver, and can only be transferred to intracellular cholesterol pool (cholesterol pool) by preventing exogenous cholesterol in the intestinal vesicles (enterocyte), inhibiting exogenous cholesterol transport to lymph, But does not affect 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.
Ezetimibe was used alone in a randomized, 190 case with hypercholesterolemia Double-blind trial, compared with the daily oral ezetimibe Ezetimibe 1, 6, the $number, 400mg kg-1, continuous treatment of 8 weeks of efficacy, found ezetimibe ezetimibe treatment of patients with plasma LDL dose-dependent reduction, Compared with baseline level, the range of LDL reduction was 0.6%-15.5%, and the total cholesterol decreased significantly; randomized, double-blind, blank control and parallel Group control study the effect of Ezetimibe ezetimibe l0mg d-1 on plasma lipids in patients with primary hypercholesterolemia, and confirmed that this product can significantly reduce the level of ldi-c. Ⅱ, Ⅲ clinical trials showed that ezetimibe Ezetimibe had good safety and tolerability, and found that the best curative effect was l0mg d-1, which could reduce the LDL by 18.5%, raise the HDL 3.5%, and show the trend of reducing triglyceride (-4.9%).
Studies on Pharmacodynamics and pharmacokinetics of ezetimibe ezetimibe with statins have also proved that ezetimibe ezetimibe can be used in combination with statins or bette (such as fenofibrate) for better clinical efficacy of the drug. A number of scholars have ezetimibe Ezetimibe respectively with Atorvastatin, the pharmacodynamics of Pravastatin, Lovastatin and Simvastatin were studied, and it was found that ezetimibe ezetimibe and the above 4 kinds of drugs have good synergistic effect, and the drug has good tolerability and safety, and its adverse reaction is similar to that of placebo. In pharmacokinetic studies, Ezetimibe ezetimibe had no significant effect on the metabolism of Simvastatin and atorvastatin. Since ezetimibe ezetimibe does not cause the illness of the patients with high triglyceride, it can be used alone in patients who cannot tolerate other lipid-lowering drugs, or with statins for patients who cannot tolerate high-dose statins. Clinically reported ezetimibe ezetimibe adverse reactions are slightly rare, more common is allergic reaction, the appearance of facial and lingual pharyngeal edema, may cause dyspnea and dysphagia, sometimes appear rash, occasional gastrointestinal discomfort and fatigue. In a word, ezetimibe ezetimibe is a new type of cholesterol absorption inhibitor with excellent pharmacological activity and safety, and it is a new type of pharmacological action in the field of lipid regulation, which has a wide market prospect. However, the long-term effect of ezetimibe ezetimibe on morbidity and mortality rates of cardiovascular disease remains to be further examined in the future.