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Esomeprazole, the S-optical isomer of omeprazole, is the world's first isomer proton pump inhibitor (PPI), which reduces gastric acid secretion by specifically inhibiting the gastric parietal cell proton pump. A large number of clinical experiments and drug studies have confirmed that its maintenance of gastric pH>4 for a longer time, higher acid inhibition efficiency, efficacy is better than the previous two generations of PPI, and individual differences are small. As a new generation of PPI, it has been widely used in clinical treatment of many acid-related diseases.
Gastroesophageal Reflux Disease (GERD)- Treatment of erosive reflux esophagitis - Long-term maintenance therapy to prevent recurrence in patients with cured esophagitis - Symptom control of Gastroesophageal reflux disease (GERD) in combination with appropriate antimicrobial therapy to eradicate Helicobacter pylori, And - healing duodenal ulcers associated with H. pylori infection - preventing the recurrence of peptic ulcers associated with H. pylori.
Uses of Esomeprazole sodium.
Esomeprazole sodium is a sodium salt form of esomeprazole, is a commonly used anti-ulcer drug, first developed by Astra Zeneca in Sweden, a proton pump inhibitor, proton pump inhibitor (PPI) is the treatment of peptic ulcer, gastroesophageal reflux disease and other acid-related diseases of choice. At present, there are 5 kinds of PPI commonly used in clinic: omeprazole, Lansoprazole, Rabeprazole, Pantoprazole and esomeprazole.
Omeprazole was the first PPI drug, and its efficacy in treating acid-related diseases has been unanimously recognized. Esomeprazole, an S-isomer of omeprazole, reduces gastric acid secretion through a specific rake action mechanism and acts as a specific inhibitor of proton pump in parietal cells. Due to its metabolic advantages, esomeprazole sodium has higher bioavailability and more consistent pharmacokinetics than omeprazole, resulting in an increase of drugs reaching the proton pump. The effect of gastric acid control is significantly better than other proton pump inhibitors such as lansoprazole, pantoprazole and rabeprazole.
In animal experiments, it showed dose-dependent inhibition of Na+/K+ ATPase activity on isolated rabbit gastric parietal cells with IC50 of 60 μmol/L. It is more effective than omeprazole (IC50 is 100 μmol/L). At the same time, Esomeprazole sodium also inhibited the histamine-induced accumulation of 14C aminopyrine in isolated human gastric parietal cells, and the effect was twice as strong as that of omeprazole.
The gastric acid secretion induced by histamine can be inhibited by intravenous or enteral injection of esomeprazole sodium in experimental rat models with ED50 of 0.24 and 0.43 mg/kg, respectively. The ED50 of omeprazole was 0.30 and 0.68 mg/kg, respectively.
Drug interaction of Bulk Esomeprazole sodium powder.
Esomeprazole sodium can reduce the absorption of ketoconazole and itraconazole. When used with this product, the dosage of drugs metabolized by the enzyme CYP2C19, such as Dicoxim, Citalopram, imipramine, Clomipramine and phenytoin, should be reduced. Plasma concentrations of phenytoin should be monitored when combined with or discontinued.
There is no interaction with amoxicillin, quinidine or warfarin, and no dose adjustment is required when used with clarithromycin.
There are few clinical data on overdose of this product, but a single dose of 80 mg of this product has not seen adverse reactions. There is no special antidote for this product.
Product Methods of Esomeprazole sodium.
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