Mechanism :
Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. The S- and R-isomers of omeprazole are protonated and converted in the acidic compartment of the parietal cell forming the active inhibitor, the achiral sulphonamide. By acting specifically on the proton pump, esomeprazole blocks the final step in acid production, thus reducing gastric acidity.
Indication :
- Gastro-esophageal reflux
- Esophageal gastric varices bleeding prophylaxis
- Acid peptic disease resistant to ranitidine
- Helicobacter pylori eradication
Contraindications :
Contraindicated in patients with known hypersensitivity to any component of the formulation or to substituted benzimidazoles.
Dosing :
Pediatric patients aged 12 to 17 years have established safety and effectiveness for delayed-release capsules and oral suspensions of esomeprazole magnesium during 4 to 8 weeks of erosive esophagitis healing.
Pediatric patients aged 1 to 11 years have established safety and effectiveness for delayed-release oral suspensions of esomeprazole magnesium during up to 8 weeks of erosive esophagitis healing.
Pediatric patients aged 1 month to under 1 year have established safety and effectiveness for delayed-release oral suspensions of esomeprazole magnesium during up to 6 weeks of acid-mediated gastroesophageal reflux disease with erosive esophagitis.
Pediatric patients under 1 month of age lack established safety and effectiveness for esomeprazole magnesium in acid-mediated gastroesophageal reflux disease with erosive esophagitis.
Pediatric patients aged 12 to 17 years have established safety and effectiveness for delayed-release capsules and oral suspensions of esomeprazole magnesium during 4 weeks of pyrosis and gastroesophageal reflux disease management.
Pediatric patients aged 1 to 11 years have established safety and effectiveness for delayed-release oral suspensions of esomeprazole magnesium during up to 8 weeks of pyrosis and gastroesophageal reflux disease symptom management.
Pediatric patients under 1 year of age lack established safety and effectiveness for esomeprazole magnesium in symptomatic gastroesophageal reflux disease management.
Pediatric populations lack established safety and effectiveness for esomeprazole magnesium in nonsteroidal anti-inflammatory drug-associated gastric ulcer risk reduction, Helicobacter pylori eradication for duodenal ulcer recurrence prevention, or pathological hypersecretory condition management.
Patients in the 12 to 17 age bracket presenting with erosive oesophagitis require a daily administration of 20 mg or 40 mg for a treatment window of 4 to 8 weeks.
Pediatric patients between 1 and 11 years of age weighing under 20 kg should receive 10 mg once daily across an 8-week course to facilitate the healing of erosive oesophagitis.
In individuals aged 1 to 11 years with a body mass of 20 kg or higher, the therapeutic regimen for erosive oesophagitis is 10 mg or 20 mg once per day over 8 weeks.
Infants aged 1 month to under 1 year in the 3 to 5 kg mass range who exhibit acid-mediated GERD-induced erosive oesophagitis require 2.5 mg OD for up to 6 weeks.
Infants aged 1 month to under 1 year weighing over 5 kg up to 7.5 kg presenting with acid-mediated GERD-induced erosive oesophagitis should be given 5 mg once daily for up to 6 weeks.
Infants aged 1 month to under 1 year with a body mass over 7.5 kg up to 12 kg affected by acid-mediated GERD-induced erosive oesophagitis necessitate 10 mg once daily for up to 6 weeks.
Adolescents aged 12 to 17 years diagnosed with symptomatic GERD should be prescribed 20 mg once per day for a duration of 4 weeks.
Children aged 1 to 11 years experiencing symptomatic GERD are managed with 10 mg administered once daily for up to 8 weeks.
Adverse Effect :
Headache, diarrhea, nausea, dizziness, flatulence, abdominal pain, constipation, dry mouth.
Interaction :
Warfarin: Changes in prothrombin measures have been received among patients on concomitant warfarin and esomeprazole therapy. Increases in INR and prothrombin time may lead to abnormal bleeding and even death. Patients treated with proton pump inhibitors and warfarin concomitantly may need to be monitored for increases in INR and prothrombin time.
Atazanavir: Concomitant administration of esomeprazole may reduce the plasma levels of atazanavir, thus appropriate clinical monitoring is recommended.
Drugs where gastric pH is important: Esomeprazole inhibits gastric acid secretion. Therefore, esomeprazole may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (e.g., ketoconazole, iron salts and digoxin).
Clarithromycin and Amoxicillin: Co-administration of esomeprazole, clarithromycin, and amoxicillin has resulted in increases in the plasma levels of esomeprazole and 14-hydroxyclarithromycin.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 20-50 | Dose as in normal renal function |
| 10-20 | Dose as in normal renal function |
| <10 | Dose as in normal renal function |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Unlikely to be dialysed. Dose as in normal renal function |
| HD | Not dialysed. Dose as in normal renal function |
| HDF/High flux | Unlikely to be dialysed. Dose as in normal renal function |
| CAV/VVHD | Unlikely to be dialysed. Dose as in normal renal function |
Hepatic Dose :
Mild to moderate hepatic impairment: No dosage adjustment required.
In adult patients with severe hepatic impairment: do not exceed 20 mg/day.