奥美拉唑钠

中文名称:

奥美拉唑钠

中文同义词:

5-甲氧基-2-[(4-甲氧基-3,5-二甲基-2-吡啶基)-甲基亚砜]-3H-苯并咪唑钠盐;奥美拉唑钠水合物;奥美拉唑钠盐;奥美拉唑钠OMEPRAZOLE SODIUM;6-甲氧基-2-(((4-甲氧基-3,5-二甲基吡啶-2-基)甲基)亚磺酰基)苯并[D]咪唑钠盐

英文名称:

Omeprazole sodium

英文同义词:

sodium 5-methoxy-2-[(4-methoxy-3,5-dimethyl-pyridin-2-yl)methylsulfinyl]benzoimidazole;OMEPRAZOLE SODIUM;5-methoxy-2-(((4-methoxy-3,5-dimethyl-2-pyridinyl)methyl)sulfinyl)-1h-benzimidazole sodium salt;Omeprazole powder/pellets/sodium;Omeprazole, sodium salt;odiuM 5-Methoxy-2-[(4-Methoxy-3,5-diMethyl-pyridin-2-yl)Methylsulfinyl]benzoiMidazole;1H-BenziMidazole, 6-Methoxy-2-[[(4-Methoxy-3,5-diMethyl-2-pyridinyl)Methyl]sulfinyl]-, sodiuM salt (1:1);omeprazole sodium:sodium 5-methoxy-2-((4-methoxy-3,5-dimethyl-pyridin-2-yl)methylsulfinyl)benzoIMIDAZOLE

CAS号:

95510-70-6

分子式:

C17H20N3NaO3S

分子量:

369.41

EINECS号:

623-285-9

相关类别:

医药原料药;化合物;中药对照品;医用原料;原料中间体-原料药;中间体;医药原料;科研产品-自主研发现货产品;Active Pharmaceutical Ingredients;Omeprazole;Digestive System;兽药原料药;消化系统;原料药;兽药原料;医用原料;医药原料;标准品;原料药;化学原料

Mol文件:

95510-70-6.mol

溶解度 

Freely soluble in water and in ethanol (96 per cent), soluble in propylene glycol, very slightly soluble in methylene chloride.

CAS 数据库

95510-70-6(CAS DataBase Reference)

概述

奥美拉唑钠是选择性抑制胃壁细胞膜中的H+-K+-ATP酶活性而产生强烈抑制胃酸分泌作用的质子泵抑制剂，主要用于治疗消化性溃疡、反流性食管炎、卓-艾综合症等疾病。具有亚硫酰基苯丙咪唑的化学结构，稳定性易受pH、光线、重金属离子、氧化性和还原性等多种因素的影响，尤其在酸性条件下，奥美拉唑钠的化学结构可发生破坏性变化，出现变色、聚合和沉淀等现象。

适应症

主要用于：①消化性溃疡出血、吻合口溃疡出血；②应激状态下时并发的急性胃黏膜损害、非甾体类抗炎药引起的急性胃黏膜损伤；③预防重症疾病（如脑出血、严重创伤等）应激状态及胃手术后引起的上消化道出血等；④作为当口服疗法不适用时下列病症的替代疗法：十二指肠溃疡、胃溃疡、反流性食管炎及Zollinger-Ellision综合征。

生物活性

Omeprazole (H 16868) 是一种质子泵 (proton pump) 抑制剂 (PPI)，有潜力用于胃肠道疾病的研究。Omeprazole 竞争性抑制 CYP2C19 活性，Ki 为 2 到 6 μM。Omeprazole 还抑制革兰氏阳性菌和革兰氏阴性菌生长。Omeprazole 是中性鞘磷脂酶 (N-SMase) 的抑制剂(外泌体抑制剂)。

靶点

Target Value CYP2C19 () Proton pump ()

Target

Value

CYP2C19 ()

Proton pump ()

体外研究

Omeprazole (H 16868) is a proton pump inhibitor used in the treatment of dyspepsia, peptic ulcer disease, gastroesophageal reflux disease, laryngopharyngeal reflux, and Zollinger-Ellison syndrome. Omeprazole (H 16868) virtually eliminated intragastric acidity in all patients: the median 24 hour intragastric pH rose from 1.4 to 5.3 and the mean hourly hydrogen ion activity fell from 38.50 to 1.95 mmol(mEq)/1 (p less than 0.001). This inhibition of 24 hour intragastric acidity is more profound than that previously reported with either cimetidine 1 g daily or ranitidine 300 mg daily. The pharmacokinetics of omeprazole were studied in a group of healthy male subjects after single and repeated oral doses of 30 and 60 mg. Absorption of Omeprazole (H 16868) from its enteric-coated formulation was unpredictable. There was a highly significant increase in the area under the plasma concentration time curve (AUC) after repeated dosing. Omeprazole (H 16868) increases its own relative availability following repeated dosing. This may be due to inhibition of gastric acid secretion by omeprazole which is an acid-labile compound. Omeprazole sodium is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).