Esomeprazole sodium Chemical Properties

Melting point 156 °C (approx)

Safety Information

MSDS Information

Esomeprazole sodium Usage And Synthesis

Anti-ulcer drug Esomeprazole Sodium is the sodium salt form of esomeprazole. It is a commonly used anti-ulcer drug, which was first successfully developed by the Swedish company Astra Zeneca first. It belongs to a proton pump inhibitor. The proton pump inhibitor is the primary choice for treating peptic ulcer, gastro-oesophageal reflux disease and other acid-related diseases. Currently commonly clinically used PPI include five kinds: omeprazole, lansoprazole, rabeprazole, pantoprazole and esomeprazole. As the first PPI, the omeprazole’s drug efficacy in treating acid-related diseases has been widely recognized. Esomeprazole is the S-isomer of omeprazole, which can reduce gastric acid secretion by specific targeting mechanism. It is the specific inhibitor for the proton pump inhibitor in the parietal cell. Owing to the metabolic advantage of esomeprazole, it has a higher bioavailability and more consistent pharmacokinetics than its counterpart, omeprazole sodium, increasing the drug that reaches the proton pump. Its role of gastric acid control is much better than other proton pumps inhibitors such as lansoprazole, pantoprazole, and rabeprazole.

In animal experiments, this product has a dose-dependent inhibition of the Na+/K+ ATP enzyme activity of the isolated rabbit parietal cells with an IC50 of 60 μmol/L. Its efficacy is greater than omeprazole (IC50: 100 μmol/L). Meanwhile, esomeprazole sodium can inhibit histamine-induced 14C aminopyrine accumulation in isolated human parietal cells. Its effect intensity is 2 times of omeprazole.

Intravenous or intestinal injections of esomeprazole sodium to the experimental fistulization rats can inhibit gastric acid secretion caused by histamine with the ED50 were 0.24 and 0.43 mg/kg, respectively. For omeprazole with the same way of injection, the ED50 is 0.30 and 0.68 mg/kg, respectively.

Using esomeprazole sodium in the gut of pylorus ligated rats enteral use esomeprazole sodium can reduce the basic amount of secreted gastric acid with potency three times larger than that of omeprazole. The drug can prevent and treat the stress or alcohol-induced gastric damage of experimental rats, also can prevent and treat the gastric lesions induced by acetic acid and indomethacin. Its ED50 values were 1.6 and 5.5 mg/kg, respectively. From the above results, the efficacy on ulcers of esomeprazole is greater than that of omeprazole.