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esomeprazole (Rx, OTC)Brand and Other Names:Nexium, Nexium 24HR

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule, delayed-release

  • 20mg (Rx/OTC)
  • 40mg

injection, powder for reconstitution

  • 20mg/vial
  • 40mg/vial

packets for oral suspension

  • 10mg
  • 20mg
  • 40mg
more...

GERD Without Erosive Esophagitis

20 mg PO qDay for 4 weeks; consider an additional 4 weeks of treatment if symptoms do not resolve completely in the first 4 weeks

GERD With Erosive Esophagitis

20-40 mg PO qDay for 4-8 weeks

If oral therapy inappropriate or not possible: 20-40 mg qDay IV up to 10 days; switch to PO once patient able to swallow

Maintenance: 20 mg PO qDay for up to 6 months

Helicobacter Pylori Eradication

Combination therapy (with amoxicillin and clarithromycin) for eradication of H pylori in patients with duodenal ulcer

40 mg PO qDay for 10 days, PLUS

Amoxicillin 1000 mg PO q12hr for 10 days, PLUS

Clarithromycin 500 mg PO q12hr for 10 days

Risk Reduction of NSAID-Associated Gastric Ulcer

20-40 mg PO qDay for up to 6 months

NSAID-Induced Gastric Ulcer

20 mg PO qDay for 4-8 weeks

Zollinger-Ellison Syndrome

80 mg PO divided q12hr (initial); adjust regimen to efficacy; up to 240 mg PO qDay, OR

120 mg PO q12hr administered to patients

Gastric or Duodenal Ulcers Following Therapeutic Endoscopy

IV indicated for risk reduction of rebleeding of gastric or duodenal ulcers following therapeutic endoscopy in adults

80 mg IV infused over 30 min, THEN continuous IV infusion of 8 mg/hr for total treatment duration of 72 hr

Follow IV therapy with oral acid suppressive therapy

Frequent Heartburn

OTC: 20 mg PO qDay x14 days

Hepatic Impairment

Oral administration

  • Mild to moderate (Child-Pugh A/B): No dosage adjustment required
  • Severe (Child-Pugh C): Not to exceed 20 mg/day

GERD (IV)

  • Mild to moderate (Child-Pugh A/B): No dosage adjustment required
  • Severe (Child-Pugh C): Not to exceed 20 mg/day IV

Bleeding gastric or duodenal ulcers (IV)

  • No dosage adjustment required with initial 80 mg/30 min IV dose
  • Adjust dose for continuous IV infusion
  • Mild-to-moderate (Child Pugh A/B): Not to exceed 6 mg/hr
  • Severe (Child Pugh C): Not to exceed 4 mg/hr

Administration

If patient unable to swallow capsule whole, capsule can be opened, emptied on applesauce, mixed, and swallowed immediately

Infuse intermittent IV over 10-30 minutes, OR not less than 3 minutes for IV injection

Dosage Forms & Strengths

capsule, delayed-release

  • 20mg
  • 40mg
  • 24.65 mg (strontium salt)
  • 49.3 mg (strontium salt)

injection, powder for reconstitution

  • 20mg/vial
  • 40mg/vial

packets for oral suspension

  • 10mg
  • 20mg
  • 40mg
more...

GERD Without Erosive Esophagitis

Oral

  • <1 year: Safety and efficacy not established
  • 1-12 years: 10-20 mg PO qDay for up to 8 weeks
  • >12 years: 20-40 mg PO qDay for up to 8 weeks

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

GERD With Erosive Esophagitis (Healing)

<1 month: Safety and efficacy not established

1 month to 1 year

  • 3.5 kg: 2.5 mg PO qDay for up to 6 weeks
  • >3.5-7.5 kg: 5 mg PO qDay for up to 6 weeks
  • >7.5 kg: 10 mg PO qDay for up to 6 weeks

1-12 years

  • <20 kg: 10 mg PO qDay for 8 weeks
  • ≥20 kg: 10-20 mg qDay for 8 weeks

>12 years

  • 20-40 mg PO qDay for 4-8 weeks
  • Maintenance: 20 mg PO qDay up to 6 months

Administration

If patient unable to swallow capsule whole, capsule can be opened, emptied on applesauce, mixed, and swallowed immediately

Infuse intermittent IV over 10-30 minutes, OR not less than 3 minutes for IV injection

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Interactions

Interaction Checker

esomeprazole and

No Results

     
     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

            Sort by :  
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            Adverse Effects

            >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)

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            Warnings

            Contraindications

            Hypersensitivity to esomeprazole or other proton pump inhibitors (PPIs)

            Cautions

            PPIs are possibly associated with increased incidence of Clostridium difficile-associated diarrhea (CDAD); consider diagnosis of CDAD for patients taking PPIs who have diarrhea that does not improve

            PPIs may decrease the efficacy of clopidogrel by reducing the formation of the active metabolite

            Gastric atrophy reported with long-term use of another PPI

            Severe hepatic impairment

            Relief of symptoms does not eliminate the possibility of a gastric malignancy

            Breastfeeding

            Therapy increases risk of Salmonella, Campylobacter, and other infections

            Contains enteric coated granules (acid labile); do not chew or crush; take 1 hr before meals

            Published observational studies suggest that PPI therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist, or spine; particularly with prolonged (>1 yr), high-dose therapy

            Decreased gastric acidity increases serum chromogranin A (CgA) levels and may cause false-positive diagnostic results for neuroendocrine tumors; temporarily discontinue PPIs before assessing CgA levels

            Hypomagnesemia may occur with prolonged use (ie, >1 yr; adverse effects may result and include tetany, arrhythmias, and seizures; in 25% of cases reviewed, magnesium supplementation alone did not improve low serum magnesium levels, and the PPI had to be discontinued

            Daily long-term use (e.g., longer than 3 years) may lead to malabsorption or a deficiency of cyanocobalamin

            Acute interstitial nephritis reported in patients taking proton pump inhibitors

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            Pregnancy & Lactation

            Pregnancy category: C (oral); B (IV)

            Lactation: Unknown whether esomeprazole is distributed into breast milk; discontinue drug or do not nurse

            Pregnancy Categories

            A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA:Information not available.

            more...
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            Pharmacology

            Mechanism of Action

            S-isomer of omeprazole; PPI; binds to H+/K+-exchanging ATPase (proton pump) in gastric parietal cells, resulting in blockage of acid secretion

            Absorption

            Bioavailability: PO: 89-90%; food decreases AUC by 33-53%; take 1 hr before meal

            Onset: 1-2 hr (gastric acid inhibition); within 4 wk (GERD)

            Duration (multiple dose): Gastric acid inhibition; PO: 17 hr

            Peak plasma time: PO: 1-1.6 hr

            Distribution

            Protein bound: 97%

            Vd: 16 L

            Metabolism

            Liver; extensively metabolized by hepatic P450 enzyme; major metabolic pathway is via CYP2C19; the rest is via CYP3A4

            Metabolites: 5-hydroxyesomeprazole (inactive), esomeprazole sulfone (inactive), desmethyl-esomeprazole (activity unknown)

            Enzymes inhibited: CYP2C19

            Slow metabolizers (3% of Caucasians and African-Americans) are deficient in CPY2C19 enzyme system; plasma concentration can be higher than in persons who have the enzyme

            Elimination

            Half-life: 1.2-1.5 hr

            Total body clearance: 9-16 L/hr

            Excretion: Urine (80%); feces (20%)

            Pharmacogenomics

            Metabolites of esomeprazole lack antisecretory activity

            The major part of esomeprazole’s metabolism is dependent on the CYP2C19 isoenzyme, which forms the hydroxy and desmethyl metabolites

            CYP2C19 isoenzyme exhibits polymorphism in the metabolism of esomeprazole, since some 3% of Caucasians and 15-20% of Asians lack CYP2C19 and are termed poor metabolizers

            At steady state, the ratio of AUC in poor metabolizers to AUC in the rest of the population (extensive metabolizers) is approximately 2

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            Administration

            IV Compatibilities

            Solution: NS, LR, D5W

            IV Preparation

            IV injection

            • Reconstitute contents of 1 vial with 5 mL NS
            • Store at room temp (no refrigeration required) and administer within 12 hr

            Intermittent IV infusion

            • Reconstitute 1 vial with 5 mL NS, LR, or D5W
            • Further dilute to 50 mL
            • Store at room temp (no refrigeration required) and administer within 12 hr if diluted in NS or LR, and within 6 hr if diluted in D5W

            Continuous IV infusion

            • Reconstitute two 40 mg vials with 5 mL each of 0.9% NaCl
            • Further dilute the 2 reconstituted vials in 100 mL 0.9% NaCl

            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
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            Images

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            Formulary

            FormularyPatient Discounts

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

            Adding plans allows you to:

            • View the formulary and any restrictions for each plan.
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            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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