Esomeprazole Injection

What is Esomeprazole Injection?

• Esomeprazole Injection (Nexium I.V.) is a proton pump inhibitor (PPI) used to treat gastroesophageal reflux disease in adults and children 1 month of age or older who have had damage to their esophagus and are unable to take esomeprazole by mouth.
• It is also used in adults to reduce the risk of further ulcer bleeding after an endoscopy.

Esomeprazole

Esomeprazole

Esomeprazole ball-and-stick model

What are the uses of this medicine?

Esomeprazole Injection (Nexium I.V.) is used for the:

• Short-term treatment of Gastroesophageal Reflux Disease (GERD) with erosive esophagitis (EE) in adults and pediatric patients 1 month to 17 years of age, as an alternative to oral therapy when oral Nexium is not possible or appropriate.
• Risk reduction of rebleeding of gastric or duodenal ulcers following endoscopy in adults.

How does this medicine work?

• 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 sulphenamide.
• By acting specifically on the proton pump, esomeprazole blocks the final step in acid production, thus reducing gastric acidity.
• This effect is dose-related up to a daily dose of 20 to 40 mg and leads to inhibition of gastric acid secretion.

Who Should Not Use this medicine ?

This medicine cannot be used:

• in patients with known hypersensitivity to substituted benzimidazoles or to any component of the formulation.
• in patients receiving rilpivirine-containing products.

What drug interactions can this medicine cause?

• Tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take.

Especially tell your doctor if you take:

• anticoagulants ('blood thinners') such as warfarin (Jantoven)
• certain antifungals such as itraconazole (Sporanox, Tolsura), ketoconazole, and voriconazole (Vfend)
• cilostazol
• citalopram (Celexa)
• clopidogrel (Plavix)
• dasatinib (Sprycel)
• digoxin (Lanoxin)
• diuretics ('water pills')
• erlotinib (Tarceva)
• iron supplements
• certain medications for human immunodeficiency virus (HIV) such as atazanavir (Reyataz, in Evotaz), nelfinavir (Viracept), and saquinavir (Invirase)
• methotrexate (Trexall, Xatmep)
• mycophenolate mofetil (Cellcept, Myfortic)
• rifampin (Rifadin, Rimactane)
• ritonavir (Norvir, in Kaletra)
• tacrolimus (Astagraf, Envarsus, Prograf)

Is this medicine FDA approved?

• Esomeprazole was approved for use in the United States in 2001 with similar indications as omeprazole includig peptic ulcer disease, gastroesophageal reflux disease and prevention of stress ulcers.

How should this medicine be used?

Recommended dosage: For GERD with Erosive Esophagitis:

• The recommended adult dosage is either 20 mg or 40 mg once daily by intravenous injection (no less than 3 minutes) or intravenous infusion (10 minutes to 30 minutes) for up to 10 days.
• The recommended pediatric dosage is based upon age and weight.

For Risk Reduction of Rebleeding of Gastric and Duodenal Ulcers:

• The recommended adult dosage is 80 mg administered as an intravenous infusion over 30 minutes, followed by a continuous infusion of 8 mg/hour for a total treatment duration of 72 hours.

Dosage Adjustment for Hepatic Impairment: GERD with EE:

• For patients with severe hepatic impairment, the maximum dosage is 20 mg once daily.

Risk Reduction of Rebleeding of Gastric or Duodenal Ulcers following Therapeutic Endoscopy in Adults:

• For patients with mild to moderate hepatic impairment, administered 80 mg as an intravenous infusion over 30 minutes, followed by a continuous infusion of 6 mg/hour for 71.5 hours.
• For patients with severe hepatic impairment, administered 80 mg as an intravenous infusion over 30 minutes, followed by a continuous infusion of 4 mg/hour for 71.5 hours.

Administration:

• Esomeprazole injection comes as a powder to be mixed with liquid and given intravenously by a doctor or nurse in a medical facility.
• For the treatment of GERD, esomeprazole is usually given intravenously once a day.
• For the prevention of re-bleeding after an endoscopy, esomeprazole injection is usually given as a continuous intravenous infusion for 72 hours.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Injection: 40 mg of esomeprazole as a lyophilized powder in a single-dose vial for reconstitution.

This medicine is available in fallowing brand namesː

• Nexium I.V.

What side effects can this medication cause?

The most common side effects of this medicine include:

• headache, flatulence, nausea, abdominal pain, injection site reaction, diarrhea, dry mouth, dizziness/vertigo, constipation and pruritus.

Less coomon, but serious side effects may include:

• Acute Tubulointerstitial Nephritis
• Clostridium difficile-Associated Diarrhea
• Bone Fracture
• Severe Cutaneous Adverse Reactions
• Cutaneous and Systemic Lupus Erythematosus
• Hypomagnesemia and Mineral Metabolism
• Fundic Gland Polyps

What special precautions should I follow?

• In adults, symptomatic response to therapy with Nexium I.V. does not preclude the presence of gastric malignancy. Consider additional follow-up and diagnostic testing.
• Acute tubulointerstitial nephritis (TIN) has been observed in patients taking PPIs and may occur at any point during PPI therapy. Discontinue treatment and evaluate patients.
• Nexium I.V. may be associated with an increased risk of Clostridium difficile-associated diarrhea, especially in hospitalized patients.
• Proton pump inhibitor (PPI) therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist, or spine.
• Severe cutaneous adverse reactions, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), drug reaction with eosinophilia and systemic symptoms (DRESS), and acute generalized exanthematous pustulosis (AGEP) have been reported in association with the use of PPIs. Discontinue at the first signs or symptoms of severe cutaneous adverse reactions or other signs of hypersensitivity and consider further evaluation.
• Cutaneous lupus erythematosus (CLE) and systemic lupus erythematosus (SLE) have been reported in patients taking PPIs, including esomeprazole. Discontinue Nexium I.V. and refer to specialist for evaluation.
• Avoid concomitant use of Nexium I.V. with clopidogrel. Concomitant use of clopidogrel with 40 mg esomeprazole reduces the pharmacological activity of clopidogrel. When using Nexium I.V. consider alternative anti-platelet therapy.
• Hypomagnesemia, symptomatic and asymptomatic, has been reported rarely in patients treated with PPIs for at least three months, in most cases after a year of therapy.
• Avoid concomitant use of Nexium I.V. with St. John’s Wort or rifampin.
• Serum chromogranin A (CgA) levels increase secondary to drug-induced decreases in gastric acidity. The increased CgA level may cause false positive results in diagnostic investigations for neuroendocrine tumors. temporarily stop Nexium I.V. at least 14 days before assessing CgA levels.
• Concomitant use with PPIs may elevate and/or prolong serum concentrations of methotrexate and/or its metabolite, possibly leading to toxicity. With high dose methotrexate administration, consider a temporary withdrawal of Nexium I.V.
• PPI use is associated with an increased risk of fundic gland polyps that increases with long-term use, especially beyond one year. Use the shortest duration of therapy.
• Esomeprazole is the S-isomer of omeprazole and limited data suggest that omeprazole may be present in human milk.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• confusion, drowsiness, blurred vision, tachycardia, nausea, diaphoresis, flushing, headache, dry mouth.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• No specific antidote for esomeprazole is known.
• Since esomeprazole is extensively protein bound, it is not expected to be removed by dialysis.
• In the event of overdosage, treatment should be symptomatic and supportive.

Can this medicine be used in pregnancy?

• There are no adequate and well-controlled studies with esomeprazole 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.

Can this medicine be used in children?

• The safety and effectiveness of Nexium I.V. have been established in pediatric patients 1 month to 17 years of age for the short-term treatment of GERD with EE, as an alternative to oral therapy when oral Nexium is not possible or appropriate.
• The safety and effectiveness of Nexium I.V. have not been established in patients less than 1 month of age for the treatment of GERD with EE or for risk reduction of rebleeding of gastric or duodenal ulcer following therapeutic endoscopy.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• ESOMEPRAZOLE SODIUM

Inactive ingredients:

• EDETATE DISODIUM
• SODIUM HYDROXIDE

Who manufactures and distributes this medicine?

Manufactured for:

• AstraZeneca Pharmaceuticals LP
• Wilmington, DE

What should I know about storage and disposal of this medication?

• Store at 25°C (77°F); excursions permitted to 15° to 30°C (59° to 86°F).
• Protect from light.
• Store in carton until time of use.
• Following reconstitution and administration, discard any unused portion of esomeprazole solution.

The antiulcer agents in clinical use

Proton Pump Inhibitors

• Dexlansoprazole
• Esomeprazole
• Lansoprazole
• Omeprazole
• Pantoprazole
• Rabeprazole

Selective Histamine Type 2 Receptor Antagonists or H2 Blockers

• Cimetidine
• Famotidine
• Nizatidine
• Ranitidine

• Dailymed label info on Esomeprazole Injection
• FDA Esomeprazole Injection

Esomeprazole Injection Resources
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