Gastroesophageal reflux disease: treatment of erosive reflux-esophagitis; long-term prevention of relapses in patients with cured esophagitis; symptomatic treatment of gastroesophageal reflux disease. Together with antibacterial agents for Helicobacter pylori eradication: treatment of duodenal ulcer associated with Helicobacter pylori; prevention of relapses of peptic ulcers in patients with ulcers caused by Helicobacter pylori. Treatment and prevention of ulcers caused by prolonged use of non-steroidal anti-inflammatory drugs (NSAIDs): treatment of ulcers caused by NSAID therapy prevention of gastric and duodenal ulcers in patients at risk for taking NSAIDs. Long-term prevention of repeated bleeding of stomach ulcers or duodenal ulcers after intravenous treatment. Treatment of Zollinger-Ellison syndrome.
active substance: esomeprazole;
1 vial contains esomeprazole sodium 42.5 mg, which is equivalent to esomeprazole 40 mg;
Excipients: disodium edetate, sodium hydroxide.
Ezomeprazol Dosage form
Lyophilisate for solution for injection and infusion.
Main physical and chemical properties: lyophilized porous mass or powder from white to almost white.
Ezomeprazol Pharmacotherapeutic group
Remedies for peptic ulcer and gastroesophageal reflux disease.
ATX code A02B C05.
Esomeprazole is the S-isomer of omeprazole, which inhibits the secretion of gastric acid due to a specific, directed mechanism of action. It is a specific inhibitor of the acid pump of parietal cells. Both the R- and S-isomers of omeprazole have similar pharmacological activity.
Place and mechanism of action
Esomeprazole is a weak base that concentrates and converts to the active form in the strongly acidic environment of the secretory tubules of parietal cells, where it inhibits the enzyme H + K + -ATPase – acid pump – and inhibits both basal and stimulated acid secretion.
Effect on the secretion of gastric juice
After 5 days of oral administration of 20 mg and 40 mg esomeprazole, gastric pH above 4 was maintained for an average of 13 hours and 17 hours, respectively, over a 24-hour interval in patients with symptomatic GERD (gastroesophageal reflux disease). The effect is similar regardless of whether esomeprazole is administered orally or intravenously.
The relationship between inhibition of acid secretion and exposure after oral administration of esomeprazole was demonstrated by AUC as an indirect parameter of drug concentration in blood plasma.
When intravenous esomeprazole was administered to healthy volunteers at a dose of 80 mg as a bolus infusion lasting 30 minutes, followed by long-term intravenous infusion at a rate of 8 mg / hour for 23.5 hours, gastric pH above 4 and above 6 was maintained on average for 21 hours and 11-13 hours over a 24-hour interval.
Therapeutic effect of inhibiting acid secretion
When orally administered esomeprazole at a dose of 40 mg, approximately 78% of patients with reflux esophagitis recover after 4 weeks, 93% – after 8 weeks of treatment.
Other effects associated with inhibition of acid secretion
During treatment with antisecretory drugs, serum gastrin levels increase in response to decreased acid secretion. The level of chromogranin A (CgA) also increases due to a decrease in the acidity of gastric juice. An increase in enterochromaffin-like cells, possibly associated with an increase in gastrin levels, has been observed in some patients during long-term treatment with oral esomeprazole.
Antisecretory therapy in the case when the oral route is impossible, for example:
gastroesophageal reflux disease in patients with esophagitis and / or severe symptoms of reflux;
treatment of gastric ulcers associated with non-steroidal anti-inflammatory drugs (NSAIDs);
prevention of gastric and duodenal ulcers associated with NSAID therapy in patients at risk.
Short-term maintenance of hemostasis and prevention of re-bleeding in patients after endoscopic treatment of acute bleeding due to gastric or duodenal ulcer.
Children (1 to 18 years old)
Antisecretory therapy when oral administration, such as gastroesophageal reflux disease (GERD), cannot be used in patients with erosive reflux esophagitis and / or severe reflux symptoms.
Hypersensitivity to esomeprazole, other substituted benzimidazoles or to any of the excipients of this drug.
Esomeprazole should not be used concomitantly with atazanavir, nelfinavir (see section “Interaction with other medicinal products and other forms of interaction”).