Esomeprazole is the newest proton pump inhibitor. It is available as esomeprazole magnesium oral tablet & esomeprazole sodium parenteral injection.
Mode of action: 'Proton pump inhibitors' interfere in the final stage of gastric acid production by blocking i.e forming a covalent bond to two sites of the H+, K+ -ATPase enzyme system ('proton pump') at the secretory surfaces of the gastric parietal cells. This leads to inhibition of both basal and stimulated gastric acid secretion irrespective of the stimulus. The binding to the H+, K+ -ATPase enzyme system results in an anti secretory effect of long duration persisting more than 24 hours.
Indication: Esomeprazole is indicated for the relief of heartburn and other symptoms associated with gastroesophageal reflux disease CGERD) and for the healing of erosive esophagitis, a potentially serious condition associated with GERD; acid related dyspepsia; duodenal and gastric ulcer; Zolinger-Ellison syndrome. Esomeprazole is also approved for using in combination of 'triple therapy' with amoxycillin and clarithromycin for the eradication of Helicobacter pylori infection in patients with duodenal ulcer disease .
Contra Indication: Known hypersensitivity to any component of the formulation.
Side Efects: Side·effects may include· headache, diarrhoea, abdominal pain etc .
Precaution: Exclude the possibility of malignancy when gastric ulcer is suspected and before treatment for dyspepsia. When using in 'triple therapy' refer to the prescribing information of the respective antibiotics.
Precautions & warnings: No dosage adjustment is necessary for geriatric patients; no dosage adjustment is necessary in renal insufficiency & in patients with mild to moderate liver impairment; patients with severe liver impairment, a dose of 20rng of esomeprazole should not be exceeded. In paediatric patient, safety and effectiveness have not yet been 'established.
Dosage & administrtion: By mouth: Gas tries I phage as reflux disease CGERD):
i. Symptomatic gastroesophageal reflux-20mg once daily for 4 weeks; if symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered.
ii. Healing of erosive esophagitis· 20mg or 40mg once daily for 4 to 8 weeks; patients who do not heal after 8 weeks, an additional 4·8 weeks treatment may be considered.
iii. Maintenance of healing of erosive esophagitis-20mg once daily for up to not beyond six months. Triple therapy for H. pylori eradication: Esomeprazole 40mg once daily for 10 days with Amoxycillin Igm twice daily for 10 days & Clarithromycin 500 mg twice daily for 10 days.
By injection: Duodenal ulcer, gastric ulcer, gastrointestinal lesions refractory to H2 blockers,
Zollinger Ellison syndrome: 40mg/day intravenously.
Reflux esophagitis: 20-40mg/day intravenously. (Reconstitution of solution: Injection solution is prepared by adding 5ml of 0.9% Sodium chloride for intravenous injection into the vial. IV injection must be administered intravenously over a period of at least 3 minutes).
Drug interaction: Esomeprazole appears to be a selective inhibitor of the cytochrome PASO mono-oxygenase system; there may be an effect on hepatic clearance, but there have been no reports to date of clinically relevant interactions. There is some uncertainly over the effect of esomeprazole on the oral combined contraceptive pill. Physiological changes similar to those found with omeprazole are likely to take place because of the reduction in gastric acid, which is likely to influence the bacterial colonization of tbe stomach and duodenum and also vitamin B 12 absorption.
Mode of action: 'Proton pump inhibitors' interfere in the final stage of gastric acid production by blocking i.e forming a covalent bond to two sites of the H+, K+ -ATPase enzyme system ('proton pump') at the secretory surfaces of the gastric parietal cells. This leads to inhibition of both basal and stimulated gastric acid secretion irrespective of the stimulus. The binding to the H+, K+ -ATPase enzyme system results in an anti secretory effect of long duration persisting more than 24 hours.
Indication: Esomeprazole is indicated for the relief of heartburn and other symptoms associated with gastroesophageal reflux disease CGERD) and for the healing of erosive esophagitis, a potentially serious condition associated with GERD; acid related dyspepsia; duodenal and gastric ulcer; Zolinger-Ellison syndrome. Esomeprazole is also approved for using in combination of 'triple therapy' with amoxycillin and clarithromycin for the eradication of Helicobacter pylori infection in patients with duodenal ulcer disease .
Contra Indication: Known hypersensitivity to any component of the formulation.
Side Efects: Side·effects may include· headache, diarrhoea, abdominal pain etc .
Precaution: Exclude the possibility of malignancy when gastric ulcer is suspected and before treatment for dyspepsia. When using in 'triple therapy' refer to the prescribing information of the respective antibiotics.
Precautions & warnings: No dosage adjustment is necessary for geriatric patients; no dosage adjustment is necessary in renal insufficiency & in patients with mild to moderate liver impairment; patients with severe liver impairment, a dose of 20rng of esomeprazole should not be exceeded. In paediatric patient, safety and effectiveness have not yet been 'established.
Dosage & administrtion: By mouth: Gas tries I phage as reflux disease CGERD):
i. Symptomatic gastroesophageal reflux-20mg once daily for 4 weeks; if symptoms do not resolve completely after 4 weeks, an additional 4 weeks of treatment may be considered.
ii. Healing of erosive esophagitis· 20mg or 40mg once daily for 4 to 8 weeks; patients who do not heal after 8 weeks, an additional 4·8 weeks treatment may be considered.
iii. Maintenance of healing of erosive esophagitis-20mg once daily for up to not beyond six months. Triple therapy for H. pylori eradication: Esomeprazole 40mg once daily for 10 days with Amoxycillin Igm twice daily for 10 days & Clarithromycin 500 mg twice daily for 10 days.
By injection: Duodenal ulcer, gastric ulcer, gastrointestinal lesions refractory to H2 blockers,
Zollinger Ellison syndrome: 40mg/day intravenously.
Reflux esophagitis: 20-40mg/day intravenously. (Reconstitution of solution: Injection solution is prepared by adding 5ml of 0.9% Sodium chloride for intravenous injection into the vial. IV injection must be administered intravenously over a period of at least 3 minutes).
Drug interaction: Esomeprazole appears to be a selective inhibitor of the cytochrome PASO mono-oxygenase system; there may be an effect on hepatic clearance, but there have been no reports to date of clinically relevant interactions. There is some uncertainly over the effect of esomeprazole on the oral combined contraceptive pill. Physiological changes similar to those found with omeprazole are likely to take place because of the reduction in gastric acid, which is likely to influence the bacterial colonization of tbe stomach and duodenum and also vitamin B 12 absorption.