BRAND NAMES
S-enantiomer of Omeprazole
 MECHANISM OF ACTION
Esomeprazole is a proton pump inhibitors. it decreases the amount of acid produced in the stomach by inhibition of H+/K+ ATPase located in the luminal membrane of gastric parietal cells
- Treatment of Gastroesophageal reflux disease (GERD)
- To prevent ulcer caused by NSAIDs.
- Treatment of ulcer caused by H. Pylori bacteria.
- Pathological hypersecretory conditions, including Zollinger-Ellison syndrome.
- Gastroesophageal Reflux Disease:
- Adults: 20-40mg/day for 4 to 8 weeks
- 12 to 17 Year Olds: 20-40mg/day for up to 8 weeks
- 1 to 11 Year Olds: 10-20mg/day for up to 8 weeks
- In infants 1 month to less than 1 year:
- 3-5 kg: 2.5 mg once daily for up to 6 Weeks
- 5-7,5 kg: 5 mg once daily for up to 6 Weeks
- 7,5-12 kg: 10 mg once daily for up to 6 Weeks
- Risk Reduction of NSAID Associated Gastric Ulcer: 20-40mg/day for up to 6 months
- H. pylori Eradication (Triple Therapy): Esomeprazole (40 mg) once daily + Amoxicillin (1000 mg) Twice Daily + Clarithromycin (500 mg) Twice Daily for 10 days
- Zollinger-Ellison syndrome: 40 mg twice daily
Patients with known hypersensitivity to PPIs (angioedema and anaphylaxis have occurred)
 WARNINGS AND PRECAUTIONS
- Symptomatic response to therapy does not rule out the presence of gastric malignancy
- PPI therapy may be associated with increased risk of Clostridium difficile associated diarrhea.
- Bone Fracture: Long-term and multiple daily dose PPI therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist or spine.
- Hypomagnesemia has been reported rarely with prolonged treatment with PPIs.
- Clopidogrel: Avoid concomitant use of Esomeprazole with clopidogrel, due to a reduction in plasma concentrations of the active metabolite of clopidogrel. When using Esomeprazole consider alternative antiplatelet therapy.
- Esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (eg, ketoconazole, iron salts, erlotinib, and digoxin)
- Combined inhibitor of CYP2C19 and CYP3A4 may raise esomeprazole levels
- Concomitant use of Esomeprazole and St. John’s wort or rifampin can substantially decrease Esomeprazole concentrations.
- Concomitant use of Esomeprazole and atazanavir or nelfinavir is not recommended because the plasma concentrations and therapeutic effects of those antiretroviral drugs may be reduced.
- Esomeprazole may increase the plasma levels of saquinavir. Dose reduction of saquinavir should be considered.
- Methotrexate: Concomitant use of Esomeprazole and methotrexate may increase and prolong the serum levels of methotrexate and/or its metabolite. In high-dose methotrexate administration, a temporary withdrawal of Esomeprazole may be considered in some patients.
- Warfarin: Patients treated with PPIs and warfarin concomitantly may need to be monitored for increases in INR and prothrombin time.
- Cilostazol: May increase systemic exposure of cilostazol and an active metabolite. Consider dose reduction
- Tacrolimus: May increase serum levels of Tacrolimus
 PREGNANCY AND LACTATION
- Pregnancy Category B (US), Esomeprazole should be used during pregnancy only if clearly needed.
- Nursing mothers: a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
 SIDE EFFECTS
In adults, the most frequently reported adverse reactions with Esomeprazole include headache, diarrhea, nausea, flatulence, dry mouth, abdominal pain and constipation.
In pediatric patients 1 to 17 years of age, the most frequently reported adverse reactions with Esomeprazole include headache, diarrhea, abdominal pain, nausea, and somnolence
In pediatric patients 1 month to less than 1 year of age: Abdominal pain, regurgitation, tachypnea and increased ALT.
 RELATED LINKS
|Heartburn/Gastritis/Gastric ulcer/Duodenal ulcer/Gastroesophageal reflux|
|H2 antagonists||Famotidine • Nizatidine • Ranitidine (Zantac)|
|Proton-pump inhibitors||Dexlansoprazole (Dexilant) • Esomeprazole (Nexium) • Lansoprazole (Prevacid) • Omeprazole (Losec, Prilosec) • Omeprazole/Sodium bicarbonate (Zegerid) • Pantoprazole (Controloc, Pantecta, Pantoloc, Protonix) ( • Rabeprazole (Aciphex, Pariet)|
|Other drugs||Alginic acid • Magaldrate • Sucralfate|
|Combination Regimens||Bismuth Subcitrate Potassium/Metronidazole/Tetracycline (Pylera) • Lansoprazole/Amoxicillin/Clarithromycin (Prevpac)|