Generic
Esomeprazole Sodium Injection
30 brands available in the market
At a glance
Esomeprazole Sodium Injection is a proton pump inhibitor (PPI) that reduces stomach acid production. It is used for heartburn, acid reflux, peptic ulcer, Zollinger-Ellison syndrome and erosive esophagitis when oral therapy is not possible or appropriate.
Description
Esomeprazole Sodium Injection irreversibly blocks the H+/K+-ATPase enzyme (proton pump) in gastric parietal cells, inhibiting the final step of gastric acid secretion. It is the S-isomer of omeprazole, providing longer-lasting acid control. It is administered as an injection when patients cannot take oral medication or when oral therapy is not appropriate. It is used for short-term treatment of GERD, erosive esophagitis, Zollinger-Ellison syndrome, peptic ulcer disease and NSAID-associated ulceration.
Indications
GERD (acid reflux), peptic ulcer disease, erosive esophagitis, Zollinger-Ellison syndrome, NSAID-associated ulceration, gastric and duodenal ulcers, acid-related dyspepsia, heartburn.
Therapeutic class
Proton Pump Inhibitor
Pharmacological class
Proton Pump Inhibitor (PPI)
Pharmacology
Esomeprazole Sodium Injection irreversibly inhibits the proton pump (H+/K+ ATPase) in gastric parietal cells, blocking the final step of gastric acid secretion. It is the S-isomer of omeprazole, providing faster and higher bioavailability compared to the R-isomer. When administered as an injection, it acts rapidly and provides relief from acid-related indigestion and heartburn by reducing gastric acid production and helps heal the esophageal and gastric lining.
Mechanism of action
Esomeprazole Sodium Injection irreversibly blocks the H+/K+-ATPase enzyme (proton pump) in gastric parietal cells, stopping the final step of gastric acid secretion. This reduces stomach acid production, providing relief from acid reflux, heartburn and peptic ulcers and helping heal the esophageal and gastric lining.
Dosage
Adult Dose:
- GERD (when oral therapy is not possible): 20 or 40 mg injection over at least 3 minutes or infusion over 10-30 minutes, once daily for up to 10 days. Convert to oral therapy as soon as possible.
- NSAID-associated ulceration: 20 mg/day injection over at least 3 minutes or infusion over 10-30 minutes. Convert to oral therapy as soon as possible.
- Gastric and duodenal ulcers: 80 mg infusion over 30 minutes, followed by continuous infusion of 8 mg/hour for 72 hours, then convert to oral therapy 40 mg once daily for 4 weeks.
Pediatric Dose:
- 1 month-1 year: 0.5 mg/kg IV once daily
- >1 year (<55 kg): 10 mg IV once daily
- >1 year (≥55 kg): 20 mg IV once daily
Special Populations: Elderly: No dosage adjustment needed. Severe hepatic impairment (Child-Pugh C): Do not exceed 20 mg/day. Renal impairment: No dosage adjustment needed.
Administration
Reconstitution: Each vial contains 20 or 40 mg of esomeprazole. For IV injection: Reconstitute with 5 mL normal saline and use within 12 hours. For IV infusion: Reconstitute with 5 mL normal saline, lactated Ringer's or 5% dextrose, then dilute to a final volume of 50 mL.
Administration: IV injection: Over no less than 3 minutes. Intermittent IV infusion: Over 10-30 minutes. Continuous IV infusion: Initial 80 mg over 30 minutes, then 8 mg/hour for 72 hours. Flush IV line before and after administration. Do not administer with any other drugs.
Missed dose
Missed injection doses are not relevant as it is administered in hospital by a physician. However, after conversion to oral therapy, if you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose and continue with your regular schedule. Do not double the dose.
Side effects
Common side effects (1-10%): Headache, flatulence, indigestion, nausea, abdominal pain, diarrhea, xerostomia, dizziness, constipation, somnolence, pruritus.
Rare side effects (<1%): Agranulocytosis, pancytopenia, blurred vision, pancreatitis, stomatitis, microscopic colitis, hepatic failure, hepatitis with or without jaundice, anaphylactic reaction/shock, GI candidiasis, hypomagnesemia, muscular weakness, myalgia, bone fracture, hepatic encephalopathy, taste disturbance, aggression, agitation, depression, hallucination, interstitial nephritis, gynecomastia, bronchospasm, alopecia, erythema multiforme, hyperhidrosis, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis.
Precautions & warnings
Caution in pediatric patients, pregnancy and lactation. Caution in malignancy and hepatic impairment. Increased risk of infections such as community-acquired pneumonia. Severe liver impairment (Child-Pugh C): Do not exceed 20 mg/day. Lactation: Discontinue drug or do not nurse.
Contraindications
Hypersensitivity to esomeprazole or substituted benzimidazoles.
Drug interactions
Avoid use with clopidogrel (reduces antiplatelet effect). Avoid with rilpivirine, atazanavir, nelfinavir (reduced bioavailability). Increases INR and prothrombin time with warfarin. Increased risk of digoxin cardiotoxicity. Increased risk of hypomagnesemia with diuretics. Other interactions: Diazepam, tacrolimus, methotrexate, ketoconazole, erlotinib, iron salts.
Food interactions
Caution advised when consuming alcohol as it may increase stomach acid production.
Use in pregnancy
There are no adequate and well-controlled studies in pregnant women. Available epidemiologic data for omeprazole fail to demonstrate an increased risk of major congenital malformations with first trimester use. Animal studies showed dose-dependent embryo-lethality. Use only if clearly needed under medical supervision.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
It is unknown whether esomeprazole is distributed into breast milk. Limited data suggest that omeprazole may be present in human milk. Discontinue drug or do not nurse during treatment.
Pediatric use
Safety and efficacy established in children (1 month-1 year: 0.5 mg/kg; >1 year weight-based dosing).
Geriatric use
No dosage adjustment needed for elderly patients.
Renal / hepatic impairment
Safe in kidney disease; no dose adjustment needed. Severe liver disease (Child-Pugh C): Do not exceed 20 mg/day.
Overdose effects
Symptoms of overdose: Drowsiness, irregular heartbeat, stomach discomfort, nausea, vomiting, headache. Seek medical attention immediately if overdose is suspected.
Storage conditions
Store below 30°C in a cool and dry place, protected from light. Use within 12 hours after reconstitution. Keep out of reach of children.
Chemical structure
Esomeprazole Sodium