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Ezetimibe It's A New Type Of Selective Cholesterol Absorption Inhibitor

Shanghai Chiral Chemicals Inc | Updated: Oct 23, 2017

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.

Hyperlipemia is one of the high risk factors of coronary heart disease, clinical treatment of hyperlipidemia mainly includes cholesterol synthesis inhibitors (such as statins), phenoxy acids (such as Bette), Bile acid chelating agents (such as the elimination of bile amines) and other (such as nicotinic acid analogues) and so on. Ezetimibe ezetimibe (Ezetim-ibe), a new cholesterol-absorbing inhibitor developed by Schering-plough and Merck Co., was approved by the FDA in October 2002 and was named Aizet (Zetia). The chemical name is (1-(4-fluorophenyl)-(3R)-& #91; 3-(4-fluorophenyl)-(3S)-Hydroxypropyl and #93;-(4S)-($number-phenyl)-(n-heterocyclic butanone), the molecular formula is c24h21 f2n03, and the relative molecular mass is 409.42.

3.1 Ezetimibe for ezetimibe alone in a randomized, double-blind trial of 190 patients with hypercholesterolemia, compared with the efficacy of daily oral ezetimibe for Ezetimibe 1, 6, $number, and 400mg·kg-1, and 8 weeks of continuous treatment, It was found that the plasma LDL of patients with ezetimibe ezetimibe was reduced in dose-dependent, and the range of LDL decreased with baseline level was 0.6%-15.5%, and the total cholesterol was significantly lower. Randomized, double-blind, blank control and parallel Group control study ezetimibe for Ezetimibe l0mg· The effect of d-1 on plasma lipids in patients with primary hypercholesterolemia confirms 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%).

3.2 The study of pharmacodynamics and pharmacokinetics of Ezetimibe ezetimibe with statins has also proved that ezetimibe ezetimibe can be used in combination with statins or bette (such as fenofibrate) for better clinical outcomes, he said. 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.