Esomeprazole Sodium 20 mg/5mL Injection — NDC 68083-451-10 (Billing 68083-0451-10)
This is a package of Esomeprazole Sodium 20 mg/5mL Injection from Gland Pharma Limited, marketed since Apr 2020 and currently FDA-listed. It is this product's only package size.
Identity & classification
Regulatory identifiers FDA, NLM and CMS codes for this package
- RxCUI (RxNorm): 486499
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 1, 2026
- RxNorm (NLM RxNav) · catalog refreshed Oct 1, 2026
- Medi-Span GPI (licensed)
- First Databank (licensed) · refreshed Oct 1, 2026
RxNorm drug class
This medicine belongs to the Proton Pump Inhibitor class.
Where does this data come from?
- RxClass (NLM) · catalog refreshed Oct 1, 2026
Clinical
- It lowers stomach acid. Doctors prescribe it for GERD, erosive esophagitis, preventing NSAID-related stomach ulcers, H. pylori infection (with antibiotics), and conditions like Zol...
- Oral forms are generally taken once a day. The over-the-counter tablet is swallowed whole with water before eating in the morning for 14 days. Follow your prescriber’s directions f...
- Not the over-the-counter versions. They can take 1 to 4 days for full effect, so they aren’t meant for immediate relief.
- Will it relieve my heartburn right away?
Patient education
Supplement & herbal interactions
Esomeprazole may be associated with lower levels of 9 nutrients — worth a chat with your pharmacist, not a cause for alarm.
Where does this data come from?
- MedlinePlus (NLM) · refreshed Oct 1, 2026
- FDA label on DailyMed · label index refreshed Oct 1, 2026
Ask a licensed pharmacist directly — free, answered by our team.
Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per each | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
Where does this data come from?
- CMS NADAC weekly file
- CMS ASP pricing files · refreshed Sep 20, 2026
- CMS Medicaid State Drug Utilization Data · refreshed Oct 2, 2026
- CMS Part D plan pricing files · refreshed Sep 24, 2026
- VA National Acquisition Center price file
Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Marketing end | Status |
|---|---|---|---|---|
| 68083-0451-10 You're viewing this Main listing | 10 VIAL in 1 CARTON / 5 mL in 1 VIAL | 2020-04-01 | — | Active |
Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Esomeprazole Sodium 20 mg/5mLthis 68083-0451-10 | Gland | 10 vials | — | — | FDA listed | — |
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- FDA Orange Book · refreshed Sep 3, 2026
- CMS NADAC weekly file
Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
- FDA Orange Book · refreshed Sep 3, 2026
Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
-
UNII 7FLD91C86K
Edetate disodium is a chemical compound that binds and removes certain metal ions. In medicines, it acts as a preservative and stabilizer by preventing metals like calcium from interfering with the product's shelf life and consistency.
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UNII 55X04QC32I
A strong alkaline chemical used to adjust and maintain the pH balance of liquid medicines. It helps keep the medicine stable and ensures it stays effective during storage.
2 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.- FDA label on DailyMed · label index refreshed Oct 1, 2026
- FDA openFDA NDC Directory · synced Oct 1, 2026
Inactive ingredient FAQ
Are inactive ingredients the same for every manufacturer?
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Manufacturer & labeler
Where does this data come from?
- FDA openFDA NDC Directory · synced Oct 1, 2026
- Drugs@FDA
Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE Esomeprazole sodium for injection is a proton pump inhibitor (PPI) indicated 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 esomeprazole sodium is not possible or appropriate. ( 1.1 ) • Risk reduction of rebleeding of gastric or duodenal ulcers following therapeutic endoscopy for acute bleeding gastric or duodenal ulcers in adults. ( 1.2 )
1.1Treatment of Gastroesophageal Reflux Disease (GERD) with Erosive Esophagitis (EE) Esomeprazole sodium for injection is indicated for the short-term treatment of GERD with EE in adults and pediatric patients 1 month to 17 years, inclusively as an alternative to oral therapy when oral esomeprazole is not possible or appropriate.
1.2Risk Reduction of Rebleeding of Gastric or Duodenal Ulcers following Therapeutic Endoscopy in Adults Esomeprazole sodium for injection is indicated for risk reduction of rebleeding of gastric or duodenal ulcers following therapeutic endoscopy for acute bleeding gastric or duodenal ulcers in adults.
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION GERD with Erosive Esophagitis ( 2.1 ): • 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. See full prescribing information. Risk Reduction of Rebleeding of Gastric and Duodenal Ulcers ( 2.2 ) : • 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 ( 2.3 ) : • See full prescribing information for dosage adjustment by severity of impairment and by indication. Preparation and Administration ( 2.4 , 2.5 ) : • See full prescribing information for preparation and administration instructions by indication.
2.1Dosage for GERD with EE Adult Patients The recommended adult dosage is either 20 mg or 40 mg esomeprazole sodium for injection given once daily by intravenous injection (over at least 3 minutes) or intravenous infusion (10 minutes to 30 minutes) for up to 10 days [see Dosage and Administration (2.4) ]. Pediatric Patients The recommended dosage for pediatric patients is based on age and body weight as shown in Table 1 below. Administer as an intravenous infusion over 10 to 30 minutes once daily for up to 10 days [ see Dosage and Administration (2.4) ].
Table 1: Recommended Pediatric Dosage Regimen for GERD with EE Age and Body Weight Dosage Regimen 1 month to less than 1 year of age 0.5 mg/kg once daily 1 year to 17 years less than 55 kg 10 mg once daily 55 kg or greater 20 mg once daily Completion of Treatment • The safety and effectiveness of esomeprazole sodium for injection for more than 10 days have not been demonstrated. • As soon as oral therapy is possible or appropriate, discontinue intravenous therapy with esomeprazole sodium for injection and continue with oral esomeprazole therapy.
2.2Dosage for Risk Reduction of Rebleeding of Gastric or Duodenal Ulcers following Therapeutic Endoscopy in Adults The recommended adult dosage is 80 mg esomeprazole sodium 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 (i.e., includes initial 30-minute loading dose plus 71.5 hours of continuous infusion) [see Dosage and Administration (2.5) ]. Intravenous therapy is aimed solely at the acute initial management of bleeding gastric or duodenal ulcers and does not constitute full treatment.
Administer oral acid-suppressive therapy following intravenous therapy for a full course of treatment.
2.3Dosage Adjustment for Hepatic Impairment GERD with EE For patients with severe hepatic impairment (Child-Pugh Class C), the maximum dosage is 20 mg once daily [see Use in Specific Populations (8.6) ]. Risk Reduction of Rebleeding of Gastric or Duodenal Ulcers following Therapeutic Endoscopy in Adults For patients with mild to moderate hepatic impairment (Child-Pugh Classes A and B, respectively), 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 (Child-Pugh Class C), administered 80 mg as an intravenous infusion over 30 minutes, followed by a continuous infusion of 4 mg/hour for 71.5 hours [see Use in Specific Populations (8.6) ].
2.4Preparation and Administration Instructions for GERD with EE Do not administer esomeprazole sodium for injection concomitantly with any other medications through the same intravenous site and/or tubing. Oral antacids may be used during treatment with esomeprazole sodium for injection. I ntravenous Injection Over At Least 3 Minutes in Adult Patients 1.
Reconstitute esomeprazole sodium for injection with 5 mL of 0.9% Sodium Chloride Injection, USP. 2. Withdraw the desired dose of the reconstituted esomeprazole… [Excerpted — this section continues on DailyMed.]
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Esomeprazole sodium for injection is 20 mg or 40 mg of esomeprazole as a white to off-white lyophilized powder in a single-dose vial for reconstitution. Esomeprazole Sodium for Injection, 20 mg or 40 mg of esomeprazole as a lyophilized powder in a single-dose vial for reconstitution. ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS • Esomeprazole sodium is contraindicated in patients with known hypersensitivity to substituted benzimidazoles or to any component of the formulation. Hypersensitivity reactions may include anaphylaxis, anaphylactic shock, angioedema, bronchospasm, acute tubulointerstitial nephritis, and urticaria [see Warnings and Precautions (5.2) , Adverse Reactions (6.2) ] . • Proton pump inhibitors (PPIs), including esomeprazole sodium for injection are contraindicated in patients receiving rilpivirine-containing products [see Drug Interactions (7) ]. • Patients with known hypersensitivity to any component of the formulation or to substituted benzimidazoles.
( 4 ) • Patients receiving rilpivirine-containing products. ( 4 , 7 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • Gastric Malignancy : In adults, symptomatic response to therapy with esomeprazole does not preclude the presence of gastric malignancy. Consider additional follow-up and diagnostic testing. ( 5.1 ) • Acute Tubulointerstitial Nephritis : Discontinue treatment and evaluate patients.
( 5.2 ) • Clostridium difficile- Associated Diarrhea : PPI therapy may be associated with increased risk. ( 5.3 ) • Bone Fracture : Long-term and multiple daily dose PPI therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist or spine. ( 5.4 ) • Severe Cutaneous Adverse Reactions : Discontinue at the first signs or symptoms of severe cutaneous adverse reactions or other signs of hypersensitivity and consider further evaluation.
( 5.5 ) • Cutaneous and Systemic Lupus Erythematosus : Mostly cutaneous; new onset or exacerbation of existing disease; discontinue esomeprazole and refer to specialist for evaluation. ( 5.6 ) • Interaction with Clopidogrel : Avoid concomitant use of esomeprazole. ( 5.7 , 7 ) • Hypomagnesemia and Mineral Metabolism: Reported rarely with prolonged treatment with PPIs.
( 5.8 ) • Interaction with St. John’s Wort or Rifampin : Avoid concomitant use of esomeprazole. ( 5.9 , 7 ) • Interactions with Diagnostic Investigations for Neuroendocrine Tumors : Increased chromogranin A (CgA) levels may interfere with diagnostic investigations for neuroendocrine tumors; temporarily stop esomeprazole at least 14 days before assessing CgA levels.
( 5.10 , 7 ) • Interaction with Methotrexate : 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 esomeprazole. ( 5.11 , 7 ) • Fundic Gland Polyps : Risk increases with long-term use, especially beyond one year.
Use the shortest duration of therapy. ( 5.12 )
5.1Presence of Gastric Malignancy In adults, symptomatic response to therapy with esomeprazole sodium for injection does not preclude the presence of gastric malignancy. Consider additional follow-up and diagnostic testing in adults patients who have suboptimal response or an early symptomatic relapse after completing treatment with a PPI. In older patients also consider an endoscopy.
5.2Acute Tubulointerstitial Nephritis Acute tubulointerstitial nephritis (TIN) has been observed in patients taking PPIs and may occur at any point during PPI therapy. Patients may present with varying signs and symptoms from symptomatic hypersensitivity reactions to nonspecific symptoms of decreased renal function (e.g., malaise, nausea, anorexia). In reported case series, some patients were diagnosed on biopsy and in the absence of extra-renal manifestations (e.g., fever, rash or arthralgia).
Discontinue esomeprazole sodium and evaluate patients with suspected acute TIN [see Contraindications (4) ].
5.3Clostridium difficile- Associated Diarrhea Published observational studies suggest that PPI therapy like esomeprazole sodium 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 [see Adverse Reactions (6.2) ]. Patients should use the lowest dose and shortest duration of PPI therapy appropriate to the condition being treated.
5.4Bone 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 establis… [Excerpted — this section continues on DailyMed.]
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following serious adverse reactions are described below and elsewhere in labeling: • Acute Tubulointerstitial Nephritis [see Warnings and Precautions (5.2) ] • Clostridium difficile -Associated Diarrhea [see Warnings and Precautions (5.3) ] • Bone Fracture [see Warnings and Precautions (5.4) ] • Severe Cutaneous Adverse Reactions [see Warnings and Precautions (5.5) ] • Cutaneous and Systemic Lupus Erythematosus [see Warnings and Precautions (5.6) ] • Hypomagnesemia and Mineral Metabolism [see Warnings and Precautions (5.8) ] • Fundic Gland Polyps [see Warnings and Precautions (5.12) ] Most common adverse reactions (≥1%) are: headache, flatulence, nausea, abdominal pain, injection site reaction, diarrhea, dry mouth, dizziness/vertigo, constipation and pruritus.
( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Gland Pharma at 864-879-9994 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
6.1Clinical 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. Symptomatic GERD and EE Adults The safety of esomeprazole sodium is based on results from clinical trials conducted in four different populations including healthy subjects (n=204) and patients with bleeding gastric or duodenal ulcers (n=375).
The data described below reflect exposure to esomeprazole sodium in 359 patients in actively-controlled trials: symptomatic GERD with or without a history of EE (n=199) and patients with EE (n=160). The population was 18 to 77 years of age; 45% Male, 52% Caucasian, 17% Black, 3% Asian, and 28% other race. Most patients received doses of either 20 or 40 mg either as an infusion or an injection.
Adverse reactions occurring in at least 1% of patients are listed below in Table 3. Table 3: Adverse Reactions 1 in the Esomeprazole Sodium Group in Active Controlled Trials of Symptomatic GERD with or without EE Adverse Reactions % of patients Esomeprazole Sodium (n=359) Headache 11 Flatulence 10 Nausea 6 Abdominal pain 6 Diarrhea 4 Mouth dry 4 Dizziness/vertigo 3 Constipation 3 Injection site reaction 2 Pruritus 1 1 Incidence of at least 1% in the esomeprazole sodium group Intravenous treatment with esomeprazole 20 and 40 mg administered as an injection or as an infusion was found to have a safety profile similar to that of oral esomeprazole.
Pediatrics A randomized, open-label, multi-national study to evaluate the pharmacokinetics of repeated intravenous doses of once daily esomeprazole in pediatric patients 1 month to 17 years old, inclusive was performed [see Clinical Pharmacology (12.3) ]. The safety results are consistent with the known safety profile of esomeprazole and no unexpected safety signals were identified. Risk Reduction of Rebleeding of Gastric or Duodenal Ulcers in Adults The data described in Table 4 below reflect exposure to esomeprazole sodium in 375 patients who presented with endoscopically confirmed gastric or duodenal ulcer bleeding in a placebo-controlled trial.
The population was 18 to 98 years old; 68% Male, 87% Caucasian, 1% Black, 7% Asian, and 4% other race. Following endoscopic hemostasis, patients received either placebo or 80 mg esomeprazole sodium as an intravenous infusion over 30 minutes followed by a continuous infusion of 8 mg/hour for a total treatment duration of 72 hours. After the initial 72-hour period, all patients received an oral PPI for 27 days.
Table 4: Adverse Reactions 1 Occurring within 72 Hours after Start of Treatment in Patients with Endoscopically Confirmed Bleeding Ulcers % of patients Esomeprazole Sodium (n=375) Placebo (n=389) Duodenal ulcer hemorrhage 4 4 Injection site reaction 2 4 1 Pyrexia 4 3 Cough 1
0.3Dizziness 1 1 1. Incidence ≥1% in the esomeprazole group and greater than placebo group 2. Injection site reactions included erythe… [Excerpted — this section continues on DailyMed.]
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Tables 5 and 6 include drugs with clinically important drug interactions and interaction with diagnostics when administered concomitantly with esomeprazole and instructions for preventing or managing them. Consult the labeling of concomitantly used drugs to obtain further information about interactions with PPIs. Table 5: Clinically Relevant Interactions Affecting Drugs Co-Administered with Esomeprazole and Interaction with Diagnostics Antiretrovirals Clinical Impact: The effect of PPIs on antiretroviral drugs is variable.
The clinical importance and the mechanisms behind these interactions are not always known. Decreased exposure of some antiretroviral drugs (e.g., rilpivirine atazanavir, and nelfinavir) when used concomitantly with esomeprazole may reduce antiviral effect and promote the development of drug resistance [see Clinical Pharmacology (12.3) ]. Increased exposure of other antiretroviral drugs (e.g., saquinavir) when used concomitantly with esomeprazole may increase toxicity [see Clinical Pharmacology (12.3) ].
There are other antiretroviral drugs which do not result in clinically relevant interactions with esomeprazole. Intervention: Rilpivirine-containing products : Concomitant use with esomeprazole sodium is contraindicated [see Contraindications (4) ] . Atazanavir : See prescribing information for atazanavir for dosing information.
Nelfinavir : Avoid concomitant use with esomeprazole sodium. See prescribing information for nelfinavir. Saquinavir : See the prescribing information for saquinavir for monitoring of potential saquinavir-related toxicities.
Other antiretrovirals : See prescribing information for specific antiretroviral drugs Warfarin Clinical Impact: Increased INR and prothrombin time in patients receiving PPIs, including esomeprazole, and warfarin concomitantly. Increases in INR and prothrombin time may lead to abnormal bleeding and even death. Intervention: Monitor INR and prothrombin time and adjust the dose of warfarin, if needed, to maintain the target INR range.
Methotrexate Clinical Impact: Concomitant use of esomeprazole with methotrexate (primarily at high dose) may elevate and prolong serum concentrations of methotrexate and/or its metabolite hydroxymethotrexate, possibly leading to methotrexate toxicities. No formal drug interaction studies of high-dose methotrexate with PPIs have been conducted [see Warnings and Precautions (5.11) ]. Intervention: A temporary withdrawal of esomeprazole sodium may be considered in some patients receiving high-dose methotrexate.
2C19 Substrates (e.g., clopidogrel, citalopram, cilostazol, diazepam) Clopidogrel Clinical Impact: Concomitant use of esomeprazole 40 mg resulted in reduced plasma concentrations of the active metabolite of clopidogrel and a reduction in platelet inhibition [see Clinical Pharmacology (12.3) ]. There are no adequate combination studies of a lower dose of esomeprazole or a higher dose of clopidogrel in comparison with the approved dose of clopidogrel . Intervention: Avoid concomitant use with esomeprazole sodium.
Consider use of alternative anti-platelet therapy [see Warnings and Precautions (5.7) ]. Citalopram Clinical Impact: Increased exposure of citalopram leading to an increased risk of QT prolongation [see Clinical Pharmacology (12.3) ]. Intervention: Limit the dose of citalopram to a maximum of 20 mg per day.
See prescribing information for citalopram. Cilostazol Clinical Impact: Increased exposure of cilostazol and one of its active metabolites (3,4-dihydro-cilostazol) [see Clinical Pharmacology (12.3) ]. Intervention: Consider reducing the dose of cilostazol to 50 mg twice daily.
See prescribing information for cilostazol. Digoxin Clinical Impact: Potential for increased exposure of digoxin [see Clinical Pharmacology (12.3) ]. Intervention: Monitor digoxin concentrations and adjust the dose, if needed, to maintain therapeutic drug concentrations.
See prescribing information for digoxin. Drugs Dependent on G… [Excerpted — this section continues on DailyMed.]
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Risk Summary 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.
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). Teratogenicity was not observed in animal reproduction studies with administration of oral esomeprazole magnesium in rats and rabbits with doses about 68 times and 42 times, respectively, an oral human dose of 40 mg (based on a body surface area basis for a 60 kg person). Changes in bone morphology were observed in offspring of rats dosed through most of pregnancy and lactation at doses equal to or greater than approximately 34 times an oral human dose of 40 mg.
When maternal administration was confined to gestation only, there were no effects on bone physeal morphology in the offspring at any age (see Data). The estimated background risks of major birth defects and miscarriage for the indicated population are unknown. All pregnancies have a background risk of birth defect, loss or other adverse outcomes.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Human Data Esomeprazole is the S-isomer of omeprazole. Four epidemiological studies compared the frequency of congenital abnormalities among infants born to women who used omeprazole during pregnancy with the frequency of abnormalities among infants of women exposed to H 2 -receptor antagonists or other controls.
A population based retrospective cohort epidemiological study from the Swedish Medical Birth Registry, covering approximately 99% of pregnancies, from 1995 to 99, reported on 955 infants (824 exposed during the first trimester with 39 of these exposed beyond first trimester, and 131 exposed after the first trimester) whose mothers used omeprazole during pregnancy. The number of infants exposed in utero to omeprazole that had any malformation, low birth weight, low Apgar score, or hospitalization was similar to the number observed in this population.
The number of infants born with ventricular septal defects and the number of stillborn infants was slightly higher in the omeprazole-exposed infants than the expected number in this population. A population-based retrospective cohort study covering all live births in Denmark from 1996 to 2009, reported on 1,800 live births whose mothers used omeprazole during the first trimester of pregnancy and 837,317 live births whose mothers did not use any proton pump inhibitor. The overall rate of birth defects in infants born to mothers with first trimester exposure to omeprazole was 2.9% and 2.6% in infants born to mothers not exposed to any proton pump inhibitor during the first trimester.
A retrospective cohort study reported on 689 pregnant women exposed to either H 2 -blockers or omeprazole in the first trimester (134 exposed to omeprazole) and 1,572 pregnant women unexposed to either during the first trimester. The overall malformation rate in offspring born to mothers with first trimester exposure to omeprazole, an H 2 -blocker, or were unexposed was 3.6%, 5.5%, and 4.1% respectively. A small prospective observational cohort study followed 113 women exposed to omeprazole during pregnancy (89% with first trimester exposures).
The reported rate of major congenital malformations was 4% in the omeprazole group, 2% in controls exposed to non-teratogens, and 2.8% in disease paired controls. Rates of spontaneous and elective abortions, preterm deliveries, gestational age at delivery, and mean birth weight were similar among t… [Excerpted — this section continues on DailyMed.]
🤰 Pregnancy ▾
8.1Pregnancy Risk Summary 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.
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). Teratogenicity was not observed in animal reproduction studies with administration of oral esomeprazole magnesium in rats and rabbits with doses about 68 times and 42 times, respectively, an oral human dose of 40 mg (based on a body surface area basis for a 60 kg person). Changes in bone morphology were observed in offspring of rats dosed through most of pregnancy and lactation at doses equal to or greater than approximately 34 times an oral human dose of 40 mg.
When maternal administration was confined to gestation only, there were no effects on bone physeal morphology in the offspring at any age (see Data). The estimated background risks of major birth defects and miscarriage for the indicated population are unknown. All pregnancies have a background risk of birth defect, loss or other adverse outcomes.
In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Human Data Esomeprazole is the S-isomer of omeprazole. Four epidemiological studies compared the frequency of congenital abnormalities among infants born to women who used omeprazole during pregnancy with the frequency of abnormalities among infants of women exposed to H 2 -receptor antagonists or other controls.
A population based retrospective cohort epidemiological study from the Swedish Medical Birth Registry, covering approximately 99% of pregnancies, from 1995 to 99, reported on 955 infants (824 exposed during the first trimester with 39 of these exposed beyond first trimester, and 131 exposed after the first trimester) whose mothers used omeprazole during pregnancy. The number of infants exposed in utero to omeprazole that had any malformation, low birth weight, low Apgar score, or hospitalization was similar to the number observed in this population.
The number of infants born with ventricular septal defects and the number of stillborn infants was slightly higher in the omeprazole-exposed infants than the expected number in this population. A population-based retrospective cohort study covering all live births in Denmark from 1996 to 2009, reported on 1,800 live births whose mothers used omeprazole during the first trimester of pregnancy and 837,317 live births whose mothers did not use any proton pump inhibitor. The overall rate of birth defects in infants born to mothers with first trimester exposure to omeprazole was 2.9% and 2.6% in infants born to mothers not exposed to any proton pump inhibitor during the first trimester.
A retrospective cohort study reported on 689 pregnant women exposed to either H 2 -blockers or omeprazole in the first trimester (134 exposed to omeprazole) and 1,572 pregnant women unexposed to either during the first trimester. The overall malformation rate in offspring born to mothers with first trimester exposure to omeprazole, an H 2 -blocker, or were unexposed was 3.6%, 5.5%, and 4.1% respectively. A small prospective observational cohort study followed 113 women exposed to omeprazole during pregnancy (89% with first trimester exposures).
The reported rate of major congenital malformations was 4% in the omeprazole group, 2% in controls exposed to non-teratogens, and 2.8% in disease paired controls. Rates of spontaneous and elective abortions, preterm deliveries, gestational age at delivery, and mean birth weight were similar among the groups. Several studies hav… [Excerpted — this section continues on DailyMed.]
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of esomeprazole sodium 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 esomeprazole is not possible or appropriate. Use of esomeprazole sodium in this age group is based on extrapolation of adult efficacy to children and the selection of dose based on exposure-matching of pediatrics to adults supported by the following evidence: a) results observed from a pharmacokinetic (PK) study on esomeprazole sodium for injection in pediatric patients, b) predictions from a population PK model comparing I.V.
PK data between adult and pediatric patients, and c) relationship between exposure and pharmacodynamic results obtained from adult I.V. and pediatric oral data and d) PK results from adequate and well-controlled studies that supported the approval of esomeprazole sodium in adults [see Adverse Reactions (6.1) , Clinical Pharmacology (12.3) , Clinical Studies (14.1) ]. The safety and effectiveness of esomeprazole sodium 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.
Juvenile Animal Data In a juvenile rat toxicity study, esomeprazole was administered with both magnesium and strontium salts at oral doses about 34 to 68 times a daily human dose of 40 mg based on body surface area. Increases in death were seen at the high dose, and at all doses of esomeprazole, there were decreases in body weight, body weight gain, femur weight and femur length, and decreases in overall growth [see Nonclinical Toxicology (13.2) ].
🧓 Geriatric Use ▾
8.5Geriatric Use In a clinical trial of patients with bleeding gastric or duodenal ulcers, 52% of 375 patients randomized to esomeprazole were 65 years of age and over. No overall differences in safety and efficacy were observed between the elderly and younger individuals, and other reported clinical experience with esomeprazole sodium for injection and oral esomeprazole has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
🆘 Overdosage ▾
10 OVERDOSAGE The symptoms described in connection with deliberate esomeprazole overdose (limited experience of doses in excess of 240 mg/day) are transient. Reports of overdosage with omeprazole in humans may also be relevant. Doses ranged up to 2,400 mg (120 times the usual recommended clinical dose).
Manifestations were variable, but included confusion, drowsiness, blurred vision, tachycardia, nausea, diaphoresis, flushing, headache, dry mouth, and other adverse reactions similar to those seen at recommended dosages. See the full prescribing information for oral omeprazole for complete safety information. 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. If over-exposure occurs, call your Poison Control Center at 1-800-222-1222 for current information on the management of poisoning or overdosage.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Esomeprazole belongs to a class of antisecretory compounds, the substituted benzimidazoles, that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase enzyme system at the secretory surface of the gastric parietal cell. Esomeprazole is protonated and converted in the acidic compartment of the parietal cell forming the active inhibitor, the achiral sulphenamide. Because this enzyme system is regarded as the acid (proton) pump within the gastric mucosa, esomeprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production.
This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus.
12.2Pharmacodynamics Antisecretory Activity The effect of esomeprazole on 24-hour intragastric pH in healthy subjects was evaluated in two studies of 20 mg and 40 mg esomeprazole sodium for injection infused intravenously once daily over 30 minutes for 5 days, as shown in Table 7. Table 7: Effect of Esomeprazole Sodium on Intragastric pH on Day 5 Esomeprazole Sodium 20 mg once daily (n=22) Esomeprazole Sodium 40 mg once daily (n=38) % Time Gastric pH>4 49.5 66.2 (95% CI) 41.9 to 57.2 62.4 to
70.0Gastric p H was measured over a 24-hour period The effects of esomeprazole on 24-hour intragastric pH following administration of an intravenous infusion of 80 mg esomeprazole sodium for injection over 30 minutes followed by a continuous infusion of 8 mg/hour for 23.5 hours was evaluated in two studies. In H. pylor i-negative healthy Caucasian subjects (n=24), the % time over 24 hours (95% CI) when the intragastric pH was > 6 and > 7 was 52.3 % (40.3, 64.4) and 4.8 % (1.8, 7.8), respectively. In H. pylori -positive (n=8) and H. pylori- negative (n=11) healthy Chinese subjects, the % time over 24 hours (95% CI) when intragastric pH was > 6 and > 7 was 53% (45.6, 60.3) and 15.1% (9.5, 20.7).
The percentage of time with intragastric pH > 6 [59% vs. 47%] and with pH > 7 [17% vs. 11%] tended to be larger in the H. pylori positive subjects compared to H. pylori -negative subjects.
Serum Gastrin Effects The effect of esomeprazole on serum gastrin concentrations was evaluated in approximately 2,700 patients in clinical trials of oral esomeprazole for up to 8 weeks and in over 1,300 patients treated for up to 12 months. The mean fasting gastrin level increased in a dose-related manner. The increase in serum gastrin concentrations reached a plateau within two to three months of therapy and returned to baseline levels within four weeks after discontinuation of therapy.
Increased gastrin causes enterochromaffin-like cell hyperplasia and increased serum Chromogranin A (CgA) levels. The increased CgA levels may cause false positive results in diagnostic investigations for neuroendocrine tumors [see Warnings and Precautions (5.9) ]. Enterochromaffin-like (ECL) Cell Effects There are no data available on the effects of intravenous esomeprazole on ECL cells.
Human gastric biopsy specimens have been obtained from more than 3,000 patients (both children and adults) treated orally with omeprazole in long-term clinical trials. The incidence of ECL cell hyperplasia in these studies increased with time; however, no case of ECL cell carcinoids, dysplasia, or neoplasia has been found in these patients [see Nonclinical Toxicology (13.1) ]. In over 1,000 patients treated with oral esomeprazole (10 mg, 20 mg or 40 mg/day) for up to 12 months, the prevalence of ECL cell hyperplasia increased with time and dose.
No patient developed ECL cell carcinoids, dysplasia, or neoplasia in the gastric mucosa. Endocrine Effects Esomeprazole had no effect on thyroid function when given in oral doses of 20 mg or 40 mg for 4 weeks. Other effects of esomeprazole on the endocrine system were assessed in studies of omeprazole.
Oral doses of omeprazole 30 mg or 40 mg per day for 2 to 4 weeks had no effect on carbohydrat… [Excerpted — this section continues on DailyMed.]
🧬 Mechanism of Action ▾
12.1Mechanism of Action Esomeprazole belongs to a class of antisecretory compounds, the substituted benzimidazoles, that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase enzyme system at the secretory surface of the gastric parietal cell. Esomeprazole is protonated and converted in the acidic compartment of the parietal cell forming the active inhibitor, the achiral sulphenamide. Because this enzyme system is regarded as the acid (proton) pump within the gastric mucosa, esomeprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production.
This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING Esomeprazole Sodium for Injection is supplied in a single-dose vial as a white to off-white lyophilized powder for reconstitution containing 20 mg or 40 mg of esomeprazole. Esomeprazole Sodium for Injection is available as follows: Product Name NDC No. Pack configuration Esomeprazole Sodium for Injection, 20 mg/vial 68083-451-10 Ten single dose 5 mL vials in one carton Esomeprazole Sodium for Injection, 40 mg/vial 68083-452-10 Ten single dose 5 mL vials in one carton Storage Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].
Protect from light. Store in carton until time of use. Following reconstitution and administration, discard any unused portion of esomeprazole solution. [see Dosage and Administration (2.4 , 2.5 )].
📋 Description ▾
11 DESCRIPTION The active ingredient in Esomeprazole Sodium for Injection is ( S )-5-methoxy-2[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]sulfinyl]-1 H -benzimidazole sodium, a PPI. Esomeprazole is the S-isomer of omeprazole, which is a mixture of the S- and R-isomers. Its empirical formula is C 17 H 18 N 3 O 3 SNa with molecular weight of 367.4 g/mol (sodium salt) and 345.4 g/mol (parent compound).
Esomeprazole sodium is very soluble in water and freely soluble in ethanol (95%). The structural formula is: Esomeprazole sodium for injection is supplied as a sterile, lyophilized, white to off-white, porous cake or powder in a 5 mL single-dose vial, intended for intravenous administration after reconstitution with 0.9% Sodium Chloride Injection, USP; Lactated Ringer’s Injection, USP or 5% Dextrose Injection, USP. Esomeprazole sodium for injection contains esomeprazole sodium 21.3 mg or 42.5 mg equivalent to esomeprazole 20 mg or 40 mg, edetate disodium 1.5 mg and sodium hydroxide q.s. for pH adjustment.
The pH of reconstituted solution of esomeprazole sodium for injection depends on the reconstitution volume and is in the pH range of 9 to 11. The stability of esomeprazole sodium in aqueous solution is strongly pH dependent. The rate of degradation increases with decreasing pH. esomeprazole-spl-structure
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Adverse Reactions Advise patients to report to their healthcare provider if they experience any signs or symptoms consistent with: • Hypersensitivity Reactions [see Contraindications (4) ] • Acute Tubulointerstitial Nephritis [see Warnings and Precautions (5.2) ] • Clostridium difficile -Associated Diarrhea [see Warnings and Precautions (5.3) ] • Bone Fracture [see Warnings and Precautions (5.4) ] • Severe Cutaneous Adverse Reactions [see Warnings and Precautions (5.5) ] • Cutaneous and Systemic Lupus Erythematosus [see Warnings and Precautions (5.6) ] • Hypomagnesemia and Mineral Metabolism [see Warnings and Precautions (5.8) ] Drug Interactions Advise patients to report to their healthcare provider before they start treatment with any of the following: • Rilpivirine-containing products [see Contraindications (4) ] • Clopidogrel [see Warnings and Precautions (5.7) ] • St.
John’s Wort or rifampin [see Warnings and Precautions (5.9) ] • High-dose methotrexate [see Warnings and Precautions (5.11) ] Administration • Inform patients that antacids may be used while taking esomeprazole. Manufactured by: Gland Pharma Limited Hyderabad - 500043, India Revised:07/2023
🧬 Pharmacokinetics ▾
12.3Pharmacokinetics Absorption The pharmacokinetics of esomeprazole in healthy subjects following administration of esomeprazole sodium for injection 20 mg and 40 mg once daily as intravenous infusion over 30 minutes for 5 days are shown in Table 8. Table 8: Geometric Mean (95% CI) Pharmacokinetic Parameters of Esomeprazole Sodium for Injection Following Dosing for 5 Days Parameter Esomeprazole Sodium for Injection 20 mg (n=24) Esomeprazole Sodium for Injection 40 mg (n=38) AUC (micromol*h/L) 5.1 (4.0:6.6) 16.2 (14.5:18.2) C max (micromol/L) 3.9 (3.2:4.7) 7.5 (6.9:8.1) t 1/2 (h) 1.1 (0.9:1.2) 1.4 (1.3:1.5) Following intravenous administration of esomeprazole sodium for injection in 24 healthy subjects as a loading dose of 80 mg over 30 minutes followed by a continuous infusion of 8 mg/hour for 23.5 hours (for a total of 24 hours), esomeprazole pharmacokinetic parameters [geometric mean value (95% CI)] were as follows: AUCt 111.1 micromol*h/L (100.5, 122.7 micromol*h/L), C max 15.0 micromol/L (13.5, 16.6 micromol/L), and steady state plasma concentration (Css) 3.9 micromol/L (3.5, 4.5 micromol/L).
In another study of healthy Caucasian subjects administered the same treatment regimen. Esomeprazole is a time-dependent inhibitor of CYP2C19, resulting in autoinhibition and nonlinear pharmacokinetics. The systemic exposure increases in a more than dose proportional manner after multiple oral doses of esomeprazole.
Compared to the first dose, the systemic exposure (C max and AUC 0-24h ) at steady state following once a day dosing increased by 43% and 90%, respectively, compared to after the first dose for the 20 mg dose and increased by 95% and 159%, respectively, for the 40 mg dose. Distribution Esomeprazole is 97% bound to plasma proteins. Plasma protein binding is constant over the concentration range of 2 to 20 micromol/L.
The apparent volume of distribution at steady state in healthy subjects is approximately 16 L. Elimination Metabolism Esomeprazole is extensively metabolized in the liver by the cytochrome P450 (CYP) enzyme system. The metabolites of esomeprazole lack antisecretory activity.
The major part of esomeprazole’s metabolism is dependent upon the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites. The remaining amount is dependent on CYP3A4 which forms the sulphone metabolite. Excretion Esomeprazole is excreted as metabolites primarily in urine but also in feces.
Less than 1% of parent drug is excreted in the urine. Esomeprazole is completely eliminated from plasma, and there is no accumulation during once daily administration. The plasma elimination half-life of esomeprazole following intravenous administration of esomeprazole sodium for injection is approximately 1.1 to 1.4 hours and is prolonged with increasing doses.
The plasma clearance (CL) is approximately 5.9 to
7.2L/h during administration of esomeprazole sodium as an intravenous infusion of 80 mg over 30 minutes followed by a continuous infusion of 8 mg/hour for 23.5 hours. Specific Populations Geriatric Patients The AUC and C max values of esomeprazole were slightly higher (25% and 18%, respectively) in the elderly as compared to younger subjects at steady state. This increase in exposure is not considered clinically relevant.
Pediatric Patients The pharmacokinetics of esomeprazole were evaluated in 50 pediatric patients birth to 17 years of age, inclusive (of which 44 pediatric patients were 1 month to 17 years) in a randomized, open-label, multi-national, multiple dose study of 20 mg esomeprazole sodium for injection administered as a once-daily 3-minute intravenous injection. Esomeprazole plasma AUC values were 183% and 60% higher in pediatric patients aged 6 to 11 years and 12 to 17 years, respectively, compared to adults. Subsequent pharmacokinetic analyses predicted the following dosage regimens would achieve comparable steady-state plasma exposures (AUC 0-24 ) to those observed in adult patients administered 20 mg of esomeprazole… [Excerpted — this section continues on DailyMed.]
🧬 Pharmacodynamics ▾
12.2Pharmacodynamics Antisecretory Activity The effect of esomeprazole on 24-hour intragastric pH in healthy subjects was evaluated in two studies of 20 mg and 40 mg esomeprazole sodium for injection infused intravenously once daily over 30 minutes for 5 days, as shown in Table 7. Table 7: Effect of Esomeprazole Sodium on Intragastric pH on Day 5 Esomeprazole Sodium 20 mg once daily (n=22) Esomeprazole Sodium 40 mg once daily (n=38) % Time Gastric pH>4 49.5 66.2 (95% CI) 41.9 to 57.2 62.4 to
70.0Gastric p H was measured over a 24-hour period The effects of esomeprazole on 24-hour intragastric pH following administration of an intravenous infusion of 80 mg esomeprazole sodium for injection over 30 minutes followed by a continuous infusion of 8 mg/hour for 23.5 hours was evaluated in two studies. In H. pylor i-negative healthy Caucasian subjects (n=24), the % time over 24 hours (95% CI) when the intragastric pH was > 6 and > 7 was 52.3 % (40.3, 64.4) and 4.8 % (1.8, 7.8), respectively. In H. pylori -positive (n=8) and H. pylori- negative (n=11) healthy Chinese subjects, the % time over 24 hours (95% CI) when intragastric pH was > 6 and > 7 was 53% (45.6, 60.3) and 15.1% (9.5, 20.7).
The percentage of time with intragastric pH > 6 [59% vs. 47%] and with pH > 7 [17% vs. 11%] tended to be larger in the H. pylori positive subjects compared to H. pylori -negative subjects.
Serum Gastrin Effects The effect of esomeprazole on serum gastrin concentrations was evaluated in approximately 2,700 patients in clinical trials of oral esomeprazole for up to 8 weeks and in over 1,300 patients treated for up to 12 months. The mean fasting gastrin level increased in a dose-related manner. The increase in serum gastrin concentrations reached a plateau within two to three months of therapy and returned to baseline levels within four weeks after discontinuation of therapy.
Increased gastrin causes enterochromaffin-like cell hyperplasia and increased serum Chromogranin A (CgA) levels. The increased CgA levels may cause false positive results in diagnostic investigations for neuroendocrine tumors [see Warnings and Precautions (5.9) ]. Enterochromaffin-like (ECL) Cell Effects There are no data available on the effects of intravenous esomeprazole on ECL cells.
Human gastric biopsy specimens have been obtained from more than 3,000 patients (both children and adults) treated orally with omeprazole in long-term clinical trials. The incidence of ECL cell hyperplasia in these studies increased with time; however, no case of ECL cell carcinoids, dysplasia, or neoplasia has been found in these patients [see Nonclinical Toxicology (13.1) ]. In over 1,000 patients treated with oral esomeprazole (10 mg, 20 mg or 40 mg/day) for up to 12 months, the prevalence of ECL cell hyperplasia increased with time and dose.
No patient developed ECL cell carcinoids, dysplasia, or neoplasia in the gastric mucosa. Endocrine Effects Esomeprazole had no effect on thyroid function when given in oral doses of 20 mg or 40 mg for 4 weeks. Other effects of esomeprazole on the endocrine system were assessed in studies of omeprazole.
Oral doses of omeprazole 30 mg or 40 mg per day for 2 to 4 weeks had no effect on carbohydrate metabolism, circulating levels of parathyroid hormone, cortisol, estradiol, testosterone, prolactin, cholecystokinin or secretin.
🔬 Clinical Studies ▾
14 CLINICAL STUDIES
14.1Acid Suppression in GERD Four multicenter, open-label, two-period crossover studies were conducted to compare the pharmacodynamic effects of esomeprazole following intravenous or oral administration on acid suppression in 206 patients with symptoms of GERD with or without erosive esophagitis. Patients were randomized to receive either 20 or 40 mg of esomeprazole sodium for injection or oral esomeprazole once daily for 10 days (Period 1), and then were switched in Period 2 to the other formulation for 10 days, matching their respective dose from Period 1.
Esomeprazole sodium for injection 20 mg and 40 mg was administered as a 3-minute injection in two of the studies and as a 15-minute infusion in the other two studies. The patient population ranged from 18 to 72 years old; 54% were female; 53% Caucasian, 24% Black, 5% Asian, and 17% other race. Basal acid output (BAO) and maximal acid output (MAO) were determined 22 to 24 hours post-dose on Period 1, Day 11; on Period 2, Day 3; and on Period 2, Day 11.
BAO and MAO were estimated from 1-hour continuous collections of gastric contents prior to and following (respectively) subcutaneous injection of 6.0 mcg/kg of pentagastrin. In these studies, after 10 days of once daily administration, esomeprazole sodium for injection, 20 mg and 40 mg were similar to the corresponding oral dosage of esomeprazole in their ability to suppress BAO and MAO in these GERD patients (see Table 9 below). There were no major changes in acid suppression when switching between intravenous and oral dosage forms.
Table 9: Mean (SD) BAO and MAO Measured 22 to 24 Hours Post-Dose Following Once Daily Oral and Intravenous Administration of Esomeprazole for 10 days in GERD Patients with or without a History of EE Study Dose in mg Intravenous Administration Method BAO in mmol H + /h MAO in mmol H + /h Intravenous Oral Intravenous Oral 1 (N=42) 20 3-minute injection 0.71 (1.24) 0.69 (1.24) 5.96 (5.41) 5.27 (5.39) 2 (N=44) 20 15-minute infusion 0.78 (1.38) 0.82 (1.34) 5.95 (4.00) 5.26 (4.12) 3 (N=50) 40 3-minute injection 0.36 (0.61) 0.31 (0.55) 5.06 (3.90) 4.41 (3.11) 4 (N=47) 40 15-minute infusion 0.36 (0.79) 0.22 (0.39) 4.74 (3.65) 3.52 (2.86)
14.2Bleeding Gastric or Duodenal Ulcers A randomized, double blind, placebo-controlled clinical study was conducted in 764 patients who presented with endoscopically confirmed gastric or duodenal ulcer bleeding. The population was 18 to 98 years old; 68% were male, 87% Caucasian, 1% Black, 7% Asian, and 4% other race. Following endoscopic hemostasis, patients were randomized to either placebo or esomeprazole sodium 80 mg as an intravenous infusion over 30 minutes followed by a continuous infusion of 8 mg/hour for a total of 72 hours.
After the initial 72-hour period, all patients received an oral PPI for 27 days. The occurrence of rebleeding within 3 days of randomization was 5.9% in the esomeprazole sodium treated group compared to 10.3% for the placebo group (treatment difference -4.4%; 95% confidence interval: -8.3%, -0.6%; p=0.03). This treatment difference was similar to that observed at Day 7 and Day 30, during which all patients were receiving an oral PPI.
A randomized, double blind, placebo-controlled single-center study conducted in Hong Kong also demonstrated a reduction compared to placebo in the risk of rebleeding within 72 hours in patients with bleeding gastric or duodenal ulcers who received racemic omeprazole, 50% of which is the S-enantiomer esomeprazole.
🧪 Nonclinical Toxicology ▾
13 NONCLINICAL TOXICOLOGY
13.1Carcinogenesis, Mutagenesis, Impairment of Fertility The carcinogenic potential of esomeprazole was assessed using omeprazole studies. In two 24-month oral carcinogenicity studies in rats, omeprazole at daily doses of 1.7, 3.4, 13.8, 44.0, and 140.8 mg/kg/day (about 0.4 to 34 times the human dose of 40 mg/day expressed on a body surface area basis) produced gastric ECL cell carcinoids in a dose-related manner in both male and female rats; the incidence of this effect was markedly higher in female rats, which had higher blood levels of omeprazole.
Gastric carcinoids seldom occur in the untreated rat. In addition, ECL cell hyperplasia was present in all treated groups of both sexes. In one of these studies, female rats were treated with 13.8 mg omeprazole/kg/day (about 3.4 times the human dose of 40 mg/day on a body surface area basis) for 1 year, then followed for an additional year without the drug.
No carcinoids were seen in these rats. An increased incidence of treatment-related ECL cell hyperplasia was observed at the end of 1 year (94% treated vs 10% controls). By the second year the difference between treated and control rats was much smaller (46% vs 26%) but still showed more hyperplasia in the treated group.
Gastric adenocarcinoma was seen in one rat (2%). No similar tumor was seen in male or female rats treated for 2 years. For this strain of rat no similar tumor has been noted historically, but a finding involving only one tumor is difficult to interpret.
A 78-week oral mouse carcinogenicity study of omeprazole did not show increased tumor occurrence, but the study was not conclusive. Esomeprazole was negative in the Ames mutation test, in the in vivo rat bone marrow cell chromosome aberration test, and the in vivo mouse micronucleus test. Esomeprazole, however, was positive in the in vitro human lymphocyte chromosome aberration test.
Omeprazole was positive in the in vitro human lymphocyte chromosome aberration test, the in vivo mouse bone marrow cell chromosome aberration test, and the in vivo mouse micronucleus test. The potential effects of esomeprazole on fertility and reproductive performance were assessed using omeprazole studies. Omeprazole at oral doses up to 138 mg/kg/day in rats (about 34 times the human dose of 40 mg/day on a body surface area basis) was found to have no effect on reproductive performance of parental animals.
13.2Animal Toxicology and/or Pharmacology Reproduction Studies Reproduction studies have been performed in rats at oral doses up to 280 mg/kg/day (about 68 times an oral human dose of 40 mg on a body surface area basis) and in rabbits at oral doses up to 86 mg/kg/day (about 42 times an oral human dose of 40 mg on a body surface area basis) and have revealed no evidence of impaired fertility or harm to the fetus due to esomeprazole [see Use in Specific Populations (8.1) ]. Juvenile Animal Study A 28-day toxicity study with a 14-day recovery phase was conducted in juvenile rats with esomeprazole magnesium at doses of 70 to 280 mg/kg/day (about 17 to 68 times a daily oral human dose of 40 mg on a body surface area basis).
An increase in the number of deaths at the high dose of 280 mg/kg/day was observed when juvenile rats were administered esomeprazole magnesium from postnatal day 7 through postnatal day 35. In addition, doses equal to or greater than 140 mg/kg/day (about 34 times a daily oral human dose of 40 mg on a body surface area basis), produced treatment-related decreases in body weight (approximately 14%) and body weight gain, decreases in femur weight and femur length, and affected overall growth. Comparable findings described above have also been observed in this study with another esomeprazole salt, esomeprazole strontium, at equimolar doses of esomeprazole.
📄 Carcinogenesis, Mutagenesis, Impairment of Fertility ▾
13.1Carcinogenesis, Mutagenesis, Impairment of Fertility The carcinogenic potential of esomeprazole was assessed using omeprazole studies. In two 24-month oral carcinogenicity studies in rats, omeprazole at daily doses of 1.7, 3.4, 13.8, 44.0, and 140.8 mg/kg/day (about 0.4 to 34 times the human dose of 40 mg/day expressed on a body surface area basis) produced gastric ECL cell carcinoids in a dose-related manner in both male and female rats; the incidence of this effect was markedly higher in female rats, which had higher blood levels of omeprazole.
Gastric carcinoids seldom occur in the untreated rat. In addition, ECL cell hyperplasia was present in all treated groups of both sexes. In one of these studies, female rats were treated with 13.8 mg omeprazole/kg/day (about 3.4 times the human dose of 40 mg/day on a body surface area basis) for 1 year, then followed for an additional year without the drug.
No carcinoids were seen in these rats. An increased incidence of treatment-related ECL cell hyperplasia was observed at the end of 1 year (94% treated vs 10% controls). By the second year the difference between treated and control rats was much smaller (46% vs 26%) but still showed more hyperplasia in the treated group.
Gastric adenocarcinoma was seen in one rat (2%). No similar tumor was seen in male or female rats treated for 2 years. For this strain of rat no similar tumor has been noted historically, but a finding involving only one tumor is difficult to interpret.
A 78-week oral mouse carcinogenicity study of omeprazole did not show increased tumor occurrence, but the study was not conclusive. Esomeprazole was negative in the Ames mutation test, in the in vivo rat bone marrow cell chromosome aberration test, and the in vivo mouse micronucleus test. Esomeprazole, however, was positive in the in vitro human lymphocyte chromosome aberration test.
Omeprazole was positive in the in vitro human lymphocyte chromosome aberration test, the in vivo mouse bone marrow cell chromosome aberration test, and the in vivo mouse micronucleus test. The potential effects of esomeprazole on fertility and reproductive performance were assessed using omeprazole studies. Omeprazole at oral doses up to 138 mg/kg/day in rats (about 34 times the human dose of 40 mg/day on a body surface area basis) was found to have no effect on reproductive performance of parental animals.
📄 Package Label / Principal Display Panel ▾
PACKAGE LABEL.PRINCIPAL DISPLAY PANEL Vial Label ( 20 mg/vial ) : NDC 68083- 451 -01 Esomeprazole Sodium for Injection 20 mg/Vial* For Intravenous Use Only Discard unused portion Single-Dose Vial Rx only Carton Label ( 20 mg/vial ): : NDC 68083- 451 -10 10 Single-Dose Vials Esomeprazole Sodium for Injection 20 mg/Vial* For Intravenous Use Only Discard unused portion Rx only NDC: Vial Label (4 0 mg/vial ) : NDC 68083- 452 -01 Esomeprazole Sodium for Injection 40 mg/Vial* For Intravenous Use Only Discard unused portion Single-Dose Vial Rx only Carton Label (4 0 mg/vial ) : NDC 68083- 452 -10 10 Single-Dose Vials Esomeprazole Sodium for Injection 40 mg/Vial* For Intravenous Use Only Discard unused portion Rx only esmoperazole-spl-20-mg-vial-label esmoperazole-spl-20-mg-carton-label esmoperazole-spl-40-mg-vial-label esmoperazole-spl-40-mg-carton-label
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