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奥美拉唑又名洛赛克,是80年代研究开发的质子泵(H~+/K~+-ATP酶)抑制性抗消化性溃疡药。其作用与H_2受体拮抗剂不同,本身为弱碱性,易浓集于壁细胞并变为喔米哌唑次磺酸和次磺酰胺,这两种物质中的硫原子可以和H~+/K~+-ATP酶的巯基以-S-S-的形式结合成酶-抑制物复合体,使酶失活,而减少胃酸分泌。它是迄今最强的胃酸分泌抑制药,并能阻断组胺、五肽胃泌素、氨甲酰胆碱等引起的胃酸分泌。另外,尚有减少胃液量,抑制幽门螺旋菌作用及升高血浆胃泌素作用。本药由小肠吸收及肝代谢,80%的代谢物由尿排泄,20%由粪排出。本药T1/2约1小时。 奥美拉唑主要用于胃及十二指肠溃疡、返流性
Omeprazole, also known as Losec, is a proton pump (H ~ + / K ~ + -ATPase) inhibitor anti-peptic ulcer drug researched and developed in the 1980s. Its role and H 2 receptor antagonist, itself weakly alkaline, easily concentrated in the parietal cells and into the mipiperazole sulfenic acid and sulfenamide, the two substances in the sulfur atoms and H ~ + The sulfhydryl group of the K + -ATPase binds to the enzyme-inhibitor complex in the form of -SS-, inactivating the enzyme and decreasing gastric acid secretion. It is by far the strongest inhibitor of gastric acid secretion, and can block histamine, pentagastrin, carbachol caused by gastric acid secretion. In addition, there are still reduced gastric juice, inhibition of Helicobacter pylori and increased role of plasma gastrin. The drug absorption by the small intestine and liver metabolism, 80% of the metabolites excreted by urine, 20% excreted. The drug T1 / 2 about 1 hour. Omeprazole is mainly used for gastric and duodenal ulcers, reflux