Esomeprazole magnesium

Использование

Antiulcerative

Определение

ChEBI: A magnesium salt resulting from the formal reaction of magnesium hydroxide with 2 mol eq. of esomeprazole. An inhibitor of gastric acid secretion, it is used for the treatment of gastro-oesophageal reflux disease, dyspepsia, peptic ulcer disease, and Zolli ger-Ellison syndrome.

Общее описание

Esomeprazole magnesium,S-bis(5-rnethoxy-2-[(S)-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole-l-yl) magnesiumtrihydrate (Nexium), is the S-enantiomer ofomeprazole. The benzimidazole PPIs contain a chiral sulfuratom that form an enantiomeric pair that is stable andinsoluble under standard conditions. The S-isomer ofomeprazole has slightly greater PPI activity, and its intrinsicclearance is approximately three times lower thanthat of R-omeprazole (15 vs. 43μL/min). The lowerclearance of S-omeprazole is related to slower metabolicclearance by the CYP2C19 isozyme. Although Romeprazoleis primarily transformed to the 5-hydroxymetabolite, the S-isomer is metabolized by O-demethylationand sulfoxidation, which contribute little to intrinsicclearance.