Esomeprazole Sodium Injection

Indications

Esomeprazole Sodium Injection is used for: Heartburn, Acid Related Dyspepsia, Peptic ulcer disease, Zollinger-Ellison syndrome, Gastroesophageal reflux disease (GERD), Helicobacter pylori infection, Erosive Esophagitis, Gouty arthritis.

Adult Dose

Intravenous Gastro-oesophageal reflux disease Adult: 20 or 40 mg by inj over at least 3 min or infusion over 10-30 min once daily for <10 days. Convert to oral therapy as soon as possible. NSAID-associated ulceration Adult: 20 mg/day by inj over at least 3 min or infusion over 10-30 min. Convert to oral therapy as soon as possible. Gastric and duodenal ulcers Adult: 80 mg infusion over 30 min followed by continuous infusion of 8 mg/hr over 72 hr, then convert to oral therapy given as 40 mg once daily for 4 wk. Elderly: No dosage adjustment needed. Hepatic impairment: Severe (Child-Pugh class C): <20 mg/day.

Child Dose

Short-term Treatment of GERD IV Short-term treatment of GERD with erosive esophagitis when oral therapy is not possible or appropriate <1 month: Safety and efficacy not established 1 month to 1 year: 0.5 mg/kg IV qDay >1 year (<55 kg): 10 mg IV qDay >1 year (?55 kg): 20 mg IV qDay

Renal Dose

Renal impairment: No dosage adjustment needed.

Administration

Reconstitution: Each single-use vial contains 20 or 40 mg of esomeprazole. For IV inj: Reconstitute each vial w/ 5 mL of normal saline and consume w/in 12 hr. For IV infusion: Reconstitute each vial w/ 5 mL of normal saline, lactated Ringer's inj or dextrose 5% inj, then further dilute the resultant solution to a final volume of 50 mL. IV Administration IV injection Injection: Over no less than 3 min Intermittent IV infusion Infuse over 10-30 min regardless of amount Flush IV line with NS, LR, or D5W prior to and after administration Do not administer with any other drugs Continuous IV infusion Administer initial 80 mg IV dose over 30 min, THEN follow with Continuous IV infusion of 8 mg/hr for total treatment duration of 72 hr

Contra Indications

Esomeprazole is contraindicated in patients with known hypersensitivity to any component of the formulation or to substituted Benzimidazoles.

Precautions

Paediatric; pregnancy, lactation. Malignancy and hepatic impairment. Increased risk of developing certain infections such as community-acquired pneumonia. For patients with severe liver impairment, a dose of 20 mg should not be exceeded. Lactation: Unknown whether esomeprazole is distributed into breast milk; discontinue drug or do not nurse

Pregnancy-Lactation

Pregnancy There are no adequate and well-controlled studies in pregnant women; esomeprazole is the S-isomer of omeprazole; available epidemiologic data fail to demonstrate an increased risk of major congenital malformations or other adverse pregnancy outcomes with first trimester omeprazole use; reproduction studies in rats and rabbits resulted in dose-dependent embryo-lethality at omeprazole doses that were approximately 3.4 to 34 times an oral human dose of 40 mg (based on a body surface area for a 60 kg person) Lactation Esomeprazole is the S-isomer of omeprazole and limited data suggest that omeprazole may be present in human milk; there are no clinical data on effects of esomeprazole on breastfed infant or on milk production; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from treatment or from underlying maternal condition

Interactions

Increased risk of digoxin-induced cardiotoxic effects. Increased risk of hypomagnesaemia w/ diuretics. May increase INR and prothrombin time w/ warfarin. May increase serum concentration of tacrolimus, saquinavir, methotrexate. May interfere the elimination of drugs metabolised by CYP2C19 (e.g. diazepam). May decrease the bioavailability of ketoconazole, erlotinib and Fe salts. Potentially Fatal: May decrease serum concentration and pharmacological effects of rilpivirine, atazanavir and nelfinavir. May decrease the antiplatelet effects of clopidogrel.

Adverse Effects

Side effects of Esomeprazole Sodium Injection : >10% Headache (2-11%) 1-10% Flatulence (10%), Indigestion (6%), Nausea (6%), Abdominal pain (1-6%), Diarrhea (2-4%), Xerostomia (3-4%), Dizziness (2-3%), Constipation (2-3%), Somnolence (1-2%), Pruritus (1%) <1% Blood and lymphatic system disorders: Agranulocytosis, pancytopenia Blurred vision, GI disorders: Pancreatitis, stomatitis, microscopic colitis Hepatobiliary disorders: Hepatic failure, hepatitis with or without jaundice Anaphylactic reaction/shock GI candidiasis Hypomagnesemia Musculoskeletal disorders: Muscular weakness, myalgia, bone fracture Nervous system disorders: Hepatic encephalopathy, taste disturbance Psychiatric disorders: Aggression, agitation, depression, hallucination Interstitial nephritis Gynecomastia Bronchospasm Skin and subcutaneous tissue disorders: Alopecia, erythema multiforme, hyperhidrosis, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis (sometimes fatal fatal)

Mechanism of Action

Esomeprazole is a PPI that suppresses gastric acid secretion by inhibiting H+/K+ ATPase in the gastric parietal cell. It is the S-isomer of omeprazole.