Esomeprazole is an ulcer-healing drug, that inhibits gastric acid by blocking the proton-pump (Hydrogen-Potassium at pase enzyme system) of the gastric perital cells. Esomeprazole is used for the short-term treatment of gastric and duodenal ulcers and in gastro-oesophageal reflux disease with severe symptoms. Also used in combination with anti bacterial for the eradication of Helicobacter pylori.
Esomeprazole Magnesium trihydrate is the derivative of Esomeprazole. It is of Synthetic origin and belongs to Sulphinyl Benzimidazol. . The Molecular Weight of Esomeprazole is 345.40.
Esomeprazole is indicated for the treatment of acid-reflux disorders including healing and maintenance of erosive esophagitis, and symptomatic gastroesophageal reflux disease (GERD), pepticulcer disease, Hpylorieradication, prevention of gastrointestinal bleeds with NSAID use, and for the long-term treatment of pathological hypersecretory conditions including Zollinger-Ellison Syndrome
Oral absorption of Esomeprazole found to 69.5% ±19.5. Plasma protien binding is 97%. and metabolism is reported Liver. Renal Excretion accounts for Urine and plasma half life is 1.2hour.
Mechanism of action
Esomeprazole exerts its stomach acid-suppressing effects by preventing the final step in gastric acid production by covalently binding to sulfhydryl groups of cysteines found on the (H+, K+)-ATPase enzyme at the secretory surface of gastric parietal cells. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. As the binding of esomeprazole to the (H+, K+)-ATPase enzyme is irreversible and new enzyme needs to be expressed in order to resume acid secretion, esomeprazole’s duration of anti secretory effect that persists longer than 24 hours.
The severe or irreversible adverse effects of Esomeprazole, which give rise to further complications include Liver damage.
The signs and symptoms that are produced after the acute over dosage of Esomeprazole include Ataxia, Tremor, Change in respiratory frequency, Intermediate Chronic Convulsion.
The symptomatic adverse reactions produced by Esomeprazole are more or less tolerable and if they become severe, they can be treated symptomatically, these include Flatulence, Dizziness, Headache, Fatigue, Diarrhea, Myalgia, Constipation, Abdominal pain, Dry mouth, Blurred vision, Rashes, Pruritus, Malaise, Arthralgia, Nausea and vomiting, Musculoskeletal pain, Dry mouth, dizziness, subacute myopathy, athralgia.
Warning / Precautions
Esomeprazole should be given with caution in patients with renal impairment, liver disease, in pregnancy and in breast-feeding. Proton-pump inhibitors may mask symptoms of gastric cancer, particular care required in those whose symptoms change and in those over 45 years of age the presence of gastric malignancy should excluded before treatment.
Store at room temperature, . Protect from Sunlight