Esomeprazole (injection)

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Esomeprazole (injection)
Adult Indications & Dosage
Pediatric Indications & Dosage
Contraindications
Warnings & Precautions
Adverse Reactions
Drug Interactions
Use in Specific Populations
Administration & Monitoring
Overdosage
Pharmacology
Clinical Studies
How Supplied
Images
Patient Counseling Information
Precautions with Alcohol
Brand Names
Look-Alike Names

Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Alonso Alvarado, M.D. [2]

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Overview

Esomeprazole (injection) is a proton pump inhibitor that is FDA approved for the treatment of gastroesophageal reflux disease (GERD), NSAID-associated gastric ulcer, H. pylori eradication, pathological hypersecretory conditions including Zollinger-Ellison syndrome. Common adverse reactions include abdominal pain, constipation, diarrhea, flatulence, nausea, xerostomia, headache, somnolence.

Adult Indications and Dosage

FDA-Labeled Indications and Dosage (Adult)

Condition 1
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Condition 2
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Off-Label Use and Dosage (Adult)

Guideline-Supported Use

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  • Developed by: (Organisation)
  • Class of Recommendation: (Class) (Link)
  • Strength of Evidence: (Category A/B/C) (Link)
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Condition 2
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  • Class of Recommendation: (Class) (Link)
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Non–Guideline-Supported Use

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Pediatric Indications and Dosage

FDA-Labeled Indications and Dosage (Pediatric)

Condition 1
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Condition 2
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Off-Label Use and Dosage (Pediatric)

Guideline-Supported Use

Condition 1
  • Developed by: (Organisation)
  • Class of Recommendation: (Class) (Link)
  • Strength of Evidence: (Category A/B/C) (Link)
  • Dosing Information/Recommendation
  • (Dosage)
Condition 2
  • Developed by: (Organisation)
  • Class of Recommendation: (Class) (Link)
  • Strength of Evidence: (Category A/B/C) (Link)
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Non–Guideline-Supported Use

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Contraindications

Warnings

Concurrent Gastric Malignancy
  • Symptomatic response to therapy with esomeprazole does not preclude the presence of gastric malignancy.
Atrophic Gastritis
  • Atrophic gastritis has been noted occasionally in gastric corpus biopsies from patients treated long-term with omeprazole, of which esomeprazole is an enantiomer.
Clostridium difficile associated diarrhea
  • Published observational studies suggest that PPI therapy like esomeprazole may be associated with an increased risk of Clostridium difficile associated diarrhea, especially in hospitalized patients. This diagnosis should be considered for diarrhea that does not improve.
  • Patients should use the lowest dose and shortest duration of PPI therapy appropriate to the condition being treated.
  • Clostridium diffficile associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents.
Interaction with Clopidogrel
  • Avoid concomitant use of esomeprazole with clopidogrel. Clopidogrel is a prodrug. Inhibition of platelet aggregation by clopidogrel is entirely due to an active metabolite. The metabolism of clopidogrel to its active metabolite can be impaired by use with concomitant medications, such as esomeprazole, that inhibit CYP2C19 activity. Concomitant use of clopidogrel with 40 mg esomeprazole reduces the pharmacological activity of clopidogrel. When using esomeprazole consider alternative anti-platelet therapy.
Bone Fracture
  • Several published observational studies suggest that proton pump inhibitor (PPI) therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist, or spine. The risk of fracture was increased in patients who received high-dose, defined as multiple daily doses, and long-term PPI therapy (a year or longer). Patients should use the lowest dose and shortest duration of PPI therapy appropriate to the condition being treated. Patients at risk for osteoporosis-related fractures should be managed according to established treatment guidelines.
Hypomagnesemia
  • 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. Serious adverse events include tetany, arrhythmias, and seizures. In most patients, treatment of hypomagnesemia required magnesium replacement and discontinuation of the PPI.
  • For patients expected to be on prolonged treatment or who take PPIs with medications such as digoxin or drugs that may cause hypomagnesemia (e.g., diuretics), health care professionals may consider monitoring magnesium levels prior to initiation of PPI treatment and periodically.
Concomitant use of Esomeprazole with St. John’s Wort or Rifampin
Interactions with Diagnostic Investigations for Neuroendocrine Tumors
  • 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. Healthcare providers should temporarily stop esomeprazole treatment at least 14 days before assessing CgA levels and consider repeating the test if initial CgA levels are high. If serial tests are performed (e.g. for monitoring), the same commercial laboratory should be used for testing, as reference ranges between tests may vary
Concomitant use of Esomeprazole with Methotrexate
  • Literature suggests that concomitant use of PPIs with methotrexate (primarily at high dose) may elevate and prolong serum levels of methotrexate and/or its metabolite, possibly leading to methotrexate toxicities. In high-dose methotrexate administration a temporary withdrawal of the PPI may be considered in some patients

Adverse Reactions

Clinical Trials Experience

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

Adults

The safety of esomeprazole was evaluated in over 15,000 patients (aged 18 to 84 years) in clinical trials worldwide including over 8,500 patients in the United States and over 6,500 patients in Europe and Canada. Over 2,900 patients were treated in long-term studies for up to 6-12 months. In general, esomeprazole was well tolerated in both short and long-term clinical trials.

The safety in the treatment of healing of erosive esophagitis was assessed in four randomized comparative clinical trials, which included 1,240 patients on esomeprazole 20 mg, 2,434 patients on esomeprazole 40 mg, and 3,008 patients on omeprazole 20 mg daily. The most frequently occurring adverse reactions (≥1%) in all three groups were headache (5.5, 5, and 3.8, respectively) and diarrhea (no difference among the three groups). Nausea, flatulence, abdominal pain, constipation, and dry mouth occurred at similar rates among patients taking esomeprazole or omeprazole.

Additional adverse reactions that were reported as possibly or probably related to esomeprazole with an incidence < 1% are listed below by body system:

The following potentially clinically significant laboratory changes in clinical trials, irrespective of relationship to esomeprazole, were reported in ≤ 1% of patients:

  • Increased creatinine.
  • Uric acid.
  • Total bilirubin.
  • Alkaline phosphatase.
  • ALT.
  • AST.
  • Hemoglobin.
  • White blood cell count.
  • Platelets.
  • Serum gastrin.
  • Potassium.
  • Sodium.
  • Thyroxine and thyroid stimulating hormone.
  • Decreases were seen in hemoglobin, white blood cell count, platelets, potassium, sodium, and thyroxine.
  • Endoscopic findings that were reported as adverse reactions include: duodenitis, esophagitis, esophageal stricture, esophageal ulceration, esophageal varices, gastric ulcer, gastritis, hernia, benign polyps or nodules, Barrett’s esophagus, and mucosal discoloration.
  • The incidence of treatment-related adverse reactions during 6-month maintenance treatment was similar to placebo. There were no differences in types of related adverse reactions seen during maintenance treatment up to 12 months compared to short-term treatment.
  • Two placebo-controlled studies were conducted in 710 patients for the treatment of symptomatic gastroesophageal reflux disease. The most common adverse reactions that were reported as possibly or probably related to esomeprazole were diarrhea (4.3%), headache (3.8%), and abdominal pain (3.8%).
Pediatrics

The safety of esomeprazole was evaluated in 316 pediatric and adolescent patients aged 1 to 17 years in four clinical trials for the treatment of symptomatic GERD. In 109 pediatric patients aged 1 to 11 years, the most frequently reported (at least 1%) treatment-related adverse reactions in these patients were diarrhea (2.8%), headache (1.9%) and somnolence (1.9%). In 149 pediatric patients aged 12 to 17 years the most frequently reported (at least 2%) treatment-related adverse reactions in these patients were headache (8.1%), abdominal pain (2.7%), diarrhea (2%), and nausea (2%).

The safety of esomeprazole was evaluated in 167 pediatric patients from birth to <1 year of age in three clinical trials. In a study that included 26 pediatric patients aged birth to 1 month there were no treatment related adverse reactions. In a study that included 43 pediatric patients age 1 to 11 months, inclusive the most frequently reported (at least 5%) adverse reactions, irrespective of causality, were irritability and vomiting. In a study that included 98 pediatric patients, age 1 to 11 months, inclusive exposed to esomeprazole for up to 6 weeks (including 39 patients randomized to the withdrawal phase), there were 4 treatment-related adverse reactions: abdominal pain (1%), regurgitation (1%), tachypnea (1%), and increased ALT (1%). No new safety concerns were identified in pediatric patients.

Combination Treatment with Amoxicillin and Clarithromycin

In clinical trials using combination therapy with esomeprazole plus amoxicillin and clarithromycin, no additional adverse reactions specific to these drug combinations were observed. Adverse reactions that occurred were limited to those observed when using esomeprazole, amoxicillin, or clarithromycin alone. The most frequently reported drug-related adverse reactions for patients who received triple therapy for 10 days were diarrhea (9.2%), taste perversion (6.6%), and abdominal pain (3.7%). No treatment-emergent adverse reactions were observed at higher rates with triple therapy than were observed with esomeprazole alone.

For more information on adverse reactions with amoxicillin or clarithromycin, refer to their package inserts, Adverse Reactions sections. In clinical trials using combination therapy with esomeprazole plus amoxicillin and clarithromycin, no additional increased laboratory abnormalities particular to these drug combinations were observed.

Postmarketing Experience

The following adverse reactions have been identified during post-approval use of NEXIUM. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure. These reports are listed below by body system:

  • Blood And Lymphatic: agranulocytosis, pancytopenia;
  • Eye: blurred vision;
  • Gastrointestinal: pancreatitis; stomatitis; microscopic colitis
  • Hepatobiliary: hepatic failure, hepatitis with or without jaundice;
  • Immune System: anaphylactic reaction/shock;
  • Infections and Infestations: GI candidiasis; Clostridium difficile associated diarrhea;
  • Metabolism and nutritional disorders: hypomagnesemia, with or without hypocalcemia and/or hypokalemia
  • Musculoskeletal and Connective Tissue: muscular weakness, myalgia, bone fracture;
  • Nervous System: hepatic encephalopathy, taste disturbance;
  • Psychiatric: aggression, agitation, depression, hallucination;
  • Renal and Urinary: interstitial nephritis;
  • Reproductive System and Breast: gynecomastia;
  • Respiratory, Thoracic, and Mediastinal: bronchospasm;
  • Skin and Subcutaneous Tissue: alopecia, erythema multiforme, hyperhidrosis, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis (some fatal).

Drug Interactions

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Drug 2

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Drug 3

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Drug 5

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Use in Specific Populations

Pregnancy

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Labor and Delivery

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Nursing Mothers

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Pediatric Use

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Geriatic Use

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Gender

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Race

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Renal Impairment

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Hepatic Impairment

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Females of Reproductive Potential and Males

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Immunocompromised Patients

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Others

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Administration and Monitoring

Administration

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Monitoring

Condition 1

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Condition 2

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Condition 3

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IV Compatibility

Solution

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Not Tested

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Variable

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Incompatible

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Y-Site

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Variable

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Incompatible

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Admixture

Compatible

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Not Tested

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Variable

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Incompatible

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Syringe

Compatible

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Not Tested

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Variable

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Incompatible

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TPN/TNA

Compatible

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Not Tested

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Variable

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Incompatible

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Overdosage

Acute Overdose

Signs and Symptoms

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Management

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Chronic Overdose

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Pharmacology

Esomeprazole (injection)
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Nonclinical Toxicology

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Clinical Studies

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How Supplied

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Storage

There is limited information regarding Esomeprazole (injection) Storage in the drug label.

Images

Drug Images

Package and Label Display Panel

Patient Counseling Information

(Patient Counseling Information)

Precautions with Alcohol

Alcohol-Esomeprazole interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.

Brand Names

There is limited information regarding Esomeprazole (injection) Brand Names in the drug label.

Look-Alike Drug Names

  • (Paired Confused Name 1a) — (Paired Confused Name 1b)
  • (Paired Confused Name 2a) — (Paired Confused Name 2b)
  • (Paired Confused Name 3a) — (Paired Confused Name 3b)

Drug Shortage Status

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References

The contents of this FDA label are provided by the National Library of Medicine.


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