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Esomeprazole

Pronunciation

Pronunciation

(es oh ME pray zol)

Index Terms

  • Esomeprazole Magnesium
  • Esomeprazole Sodium
  • Esomeprazole Strontium
  • Nexium 24HR

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Capsule Delayed Release, Oral, as magnesium [strength expressed as base]:

NexIUM: 20 mg, 40 mg [contains brilliant blue fcf (fd&c blue #1), fd&c red #40, fd&c yellow #10 (quinoline yellow)]

NexIUM 24HR: 20 mg [contains brilliant blue fcf (fd&c blue #1), fd&c red #40]

Generic: 20 mg, 40 mg

Capsule Delayed Release, Oral, as strontium:

Generic: 24.65 mg [DSC], 49.3 mg [DSC]

Packet, Oral, as magnesium [strength expressed as base]:

NexIUM: 2.5 mg (30 ea); 5 mg (30 ea); 10 mg (30 ea); 20 mg (30 ea); 40 mg (30 ea)

Solution Reconstituted, Intravenous, as sodium [strength expressed as base]:

NexIUM I.V.: 20 mg (1 ea [DSC]); 40 mg (1 ea)

Generic: 20 mg (1 ea); 40 mg (1 ea)

Tablet Delayed Release, Oral, as magnesium [strength expressed as base]:

NexIUM 24HR: 20 mg [contains fd&c blue #2 aluminum lake, fd&c red #40 aluminum lake]

Brand Names: U.S.

  • NexIUM
  • NexIUM 24HR [OTC]
  • NexIUM I.V.

Pharmacologic Category

  • Proton Pump Inhibitor
  • Substituted Benzimidazole

Pharmacology

Proton pump inhibitor suppresses gastric acid secretion by inhibition of the H+/K+-ATPase in the gastric parietal cell. Esomeprazole is the S-isomer of omeprazole.

Distribution

Vdss: 16 L

Metabolism

Hepatic via CYP2C19 primarily and (to a lesser extent) via 3A4 to hydroxy, desmethyl, and sulfone metabolites (all inactive)

Excretion

Urine (80%, primarily as inactive metabolites; <1% as active drug); feces (20%)

Clearance (with repeated dosing):

Children 1 to 5 years: 6 to 19.44 L/hour (Zhao 2006)

Children 6 to 11 years: 7.84 to 9.22 L/hour (Zhao 2006)

Adolescents 12 to 17 years: 8.36 to 15.88 L/hour (Li 2006)

Time to Peak

Oral:

Infants: Median: 3 hours

Children 1 to 5 years: 1.33 to 1.44 hours (Zhao 2006)

Children 6 to 11 years: 1.75 to 1.79 hours (Zhao 2006)

Adolescents 12 to 17 years: 1.96 to 2.04 hours (Li 2006)

Adults: 1.5 to 2 hours

Half-Life Elimination

Infants: 0.93 hours

Children 1 to 5 years: 0.42 to 0.74 hours (Zhao 2006)

Children 6 to 11 years: 0.73 to 0.88 hours (Zhao 2006)

Adolescents 12 to 17 years: 0.82 to 1.22 hours (Li 2006)

Adults: ~1 to 1.5 hours

Protein Binding

97%

Special Populations: Hepatic Function Impairment

AUC was 2-3 times higher in patients with severe hepatic impairment.

Special Populations: Elderly

AUC and Cmax were increased by 25% and 18%, respectively, following administration of esomeprazole magnesium.

Special Populations: Gender

AUC and Cmax were 13% higher in women than men following administration of esomeprazole magnesium..

Use: Labeled Indications

Oral:

Esomeprazole magnesium and esomeprazole strontium:

Gastroesophageal reflux disease (Rx only):

Healing of erosive esophagitis: Short-term (4 to 8 weeks) treatment of erosive esophagitis

Maintenance of healing of erosive esophagitis: Maintaining symptom resolution and healing of erosive esophagitis

Symptomatic gastroesophageal reflux disease: Short-term (4 to 8 weeks) treatment of symptomatic gastroesophageal reflux disease (GERD)

Helicobacter pylori eradication (Rx only): As part of a multidrug regimen for Helicobacter pylori eradication in patients with duodenal ulcer disease (active or history of within the past 5 years)

Risk reduction of nonsteroidal anti-inflammatory drug-associated gastric ulcer (Rx only): Prevention of gastric ulcers associated with continuous NSAID therapy in patients at risk (age ≥60 years and/or history of gastric ulcer)

Pathological hypersecretory conditions, including Zollinger-Ellison syndrome (Rx only): Treatment (long-term) of pathological hypersecretory conditions including Zollinger-Ellison syndrome

Canadian labeling: Additional use (not in US labeling): Oral: Treatment of nonerosive reflux disease (NERD); treatment of NSAID-induced gastric ulcers

Esomeprazole magnesium:

Heartburn (OTC labeling): Treatment of frequent heartburn (≥2 days per week).

IV: Esomeprazole sodium:

Gastroesophageal reflux disease (Rx only): Short-term (≤10 days) treatment of gastroesophageal reflux disease (GERD) with erosive esophagitis in pediatric patients 1 month to 17 years of age and adults when oral therapy is not possible or appropriate

Risk reduction of ulcer rebleeding postprocedure (Rx only): Decrease the risk of rebleeding postendoscopy for acute bleeding gastric or duodenal ulcers in adults

Contraindications

Hypersensitivity (eg, anaphylaxis, anaphylactic shock, angioedema, bronchospasm, acute interstitial nephritis, urticaria) to esomeprazole, other substituted benzimidazole proton pump inhibitors, or any component of the formulation

OTC labeling: When used for self-medication (OTC), do not use if you have trouble or pain when swallowing food; vomiting with blood, or bloody or black stools; heartburn with lightheadedness, dizziness, or sweating; chest pain or shoulder pain with shortness of breath, sweating, pain spreading to arms, neck or shoulders, or lightheadedness; frequent chest pain

Dosing: Adult

Note: Esomeprazole strontium capsules (all strengths) have been discontinued in the US for more than 1 year.

Note: All dosing is expressed in terms of esomeprazole base, regardless of the salt associated with the dosing information. Esomeprazole strontium 24.65 mg is equivalent to 20 mg of esomeprazole base; esomeprazole strontium 49.3 mg is equivalent to 40 mg of esomeprazole base.

Erosive esophagitis (healing): Oral: Esomeprazole magnesium, esomeprazole strontium: Initial: 20 to 40 mg once daily for 4 to 8 weeks; if incomplete healing, may continue for an additional 4 to 8 weeks; maintenance: 20 mg once daily (controlled studies did not extend beyond 6 months)

Heartburn (OTC labeling): 20 mg once daily for 14 days (maximum: 20 mg/day); treatment may be repeated after 4 months if needed

Nonerosive reflux disease (NERD) (Canadian labeling): Oral: Esomeprazole magnesium: Initial: 20 mg once daily for 2 to 4 weeks; lack of symptom control after 4 weeks warrants further evaluation; maintenance (in patients with successful initial therapy): 20 mg once daily as needed

Symptomatic gastroesophageal reflux: Oral: Esomeprazole magnesium, esomeprazole strontium: 20 mg once daily for 4 weeks; may consider an additional 4 weeks of treatment if symptoms do not resolve

Treatment of GERD (short-term): IV: 20 mg or 40 mg once daily. Note: Indicated only in cases where oral therapy is inappropriate or not possible; safety/efficacy ≥10 days has not been established.

Prevention of recurrent gastric or duodenal ulcer bleeding postendoscopy: IV: 80 mg over 30 minutes, followed by 8 mg/hour continuous infusion for a total of 72 hours, then 40 mg orally once daily for 27 additional days (Sung, 2009) or may follow continuous infusion with any single daily-dose oral proton pump inhibitor (PPI) for a duration dictated by the underlying etiology (Barkun, 2010). Note: The use of intermittent PPIs was found to be comparable with the use of continuous infusion PPIs in patients with high-risk endoscopic findings and may be preferred (Sachar, 2014).

Helicobacter pylori eradication: Oral:

Manufacturer labeling: Esomeprazole magnesium, esomeprazole strontium: 40 mg once daily administered with amoxicillin 1,000 mg and clarithromycin 500 mg twice daily for 10 days

American College of Gastroenterology guidelines (Chey, 2007):

Nonpenicillin allergy: 40 mg once daily administered with amoxicillin 1,000 mg and clarithromycin 500 mg twice daily for 10 to 14 days

Penicillin allergy: 40 mg once daily administered with clarithromycin 500 mg and metronidazole 500 mg twice daily for 10 to 14 days or 40 mg once daily administered with bismuth subsalicylate 525 mg and metronidazole 250 mg plus tetracycline 500 mg 4 times daily for 10 to 14 days

Canadian labeling: Esomeprazole magnesium: 20 mg twice daily for 7 days; requires combination therapy

Prevention of NSAID-induced gastric ulcers: Oral:

US labeling: Esomeprazole magnesium, esomeprazole strontium: 20 to 40 mg once daily for up to 6 months

Canadian labeling: Esomeprazole magnesium: 20 mg once daily for up to 6 months

Note: 40 mg daily did not show additional benefit over 20 mg daily in clinical trials.

Treatment of NSAID-induced gastric ulcers (Canadian labeling; off-label in US): Oral: Esomeprazole magnesium: 20 mg once daily for 4 to 8 weeks (Goldstein, 2007)

Pathological hypersecretory conditions (Zollinger-Ellison syndrome): Oral: Esomeprazole magnesium, esomeprazole strontium: 40 mg twice daily; adjust regimen to individual patient needs; doses up to 240 mg daily have been administered

Dosing: Geriatric

Refer to adult dosing.

Dosing: Pediatric

Note: Esomeprazole strontium capsules (all strengths) have been discontinued in the US for more than 1 year.

Note: All dosing is expressed in terms of esomeprazole base, regardless of the salt associated with the dosing information. Esomeprazole strontium is not recommended for use in pediatrics.

Symptomatic GERD: Oral: Esomeprazole magnesium:

Children 1 to 11 years: 10 mg once daily for up to 8 weeks; Note: Safety and efficacy of doses >1 mg/kg/day and/or therapy beyond 8 weeks have not been established.

Adolescents 12 to 17 years: 20 mg once daily for up to 4 weeks

Treatment of GERD (short-term): IV: Note: Indicated only in cases where oral therapy is inappropriate or not possible; safety/efficacy ≥10 days has not been established.

Children 1 month to <1 year: 0.5 mg/kg once daily

Children 1 to 17 years: <55 kg: 10 mg once daily; ≥55 kg: 20 mg once daily

Erosive esophagitis (healing): Oral: Esomeprazole magnesium:

Children 1 month to <1 year: Note: Safety and efficacy of doses >1.33 mg/kg/day and/or therapy beyond 6 weeks have not been established.

3 to 5 kg: 2.5 mg once daily for up to 6 weeks

>5 to 7.5 kg: 5 mg once daily for up to 6 weeks

>7.5 to 12 kg: 10 mg once daily for up to 6 weeks

Children 1 to 11 years: Note: Safety and efficacy of doses >1 mg/kg/day and/or therapy beyond 8 weeks have not been established.

<20 kg: 10 mg once daily for 8 weeks

≥20 kg: 10 to 20 mg once daily for 8 weeks

Adolescents 12 to 17 years: 20 to 40 mg once daily for 4 to 8 weeks

Nonerosive reflux disease (NERD) (Canadian labeling): Oral: Esomeprazole magnesium:

Children 1 to 11 years: 10 mg once daily for up to 8 weeks. Note: Safety and efficacy of doses >1 mg/kg/day and/or therapy beyond 8 weeks have not been established.

Adolescents 12 to 17 years: 20 mg once daily for 2 to 4 weeks; lack of symptom control after 4 weeks warrants further evaluation (safety studies do not extend beyond 8 weeks)

Dosing: Renal Impairment

Oral:

Esomeprazole magnesium: Mild-to-severe impairment: No dosage adjustment necessary.

Esomeprazole strontium:

Mild-to-moderate impairment: No dosage adjustment necessary.

Severe impairment: Use is not recommended (has not been studied).

IV: Mild-to-severe impairment: No dosage adjustment necessary.

Dosing: Hepatic Impairment

Oral:

Safety and efficacy not established in children with hepatic impairment.

Mild to moderate impairment (Child-Pugh class A or B): No dosage adjustment necessary.

Severe impairment (Child-Pugh class C): Maximum: 20 mg daily.

IV:

Treatment of GERD (short-term):

Mild to moderate impairment (Child-Pugh class A or B): No dosage adjustment necessary.

Severe impairment (Child-Pugh class C): Dose should not exceed 20 mg daily

Prevention of recurrent gastric or duodenal ulcer bleeding postendoscopy:

Mild to moderate impairment (Child-Pugh class A or B): 80 mg over 30 minutes, followed by a maximum continuous infusion of 6 mg/hour for a total of 72 hours

Severe impairment (Child-Pugh class C): 80 mg over 30 minutes, followed by a maximum continuous infusion of 4 mg/hour for a total of 72 hour

Reconstitution

Granules for oral administration: Empty the 2.5 mg or 5 mg packet into a container with 5 mL of water or empty the 10 mg, 20 mg, or 40 mg packet into a container with 15 mL of water and stir; leave 2-3 minutes to thicken.

Powder for injection:

For IV injection (≥3 minutes): Adults: Reconstitute powder with 5 mL NS.

For IV infusion (10 to 30 minutes):

Children: Initially reconstitute powder (20 mg or 40 mg) with 5 mL of NS, LR, or D5W, then further dilute to a final volume of 50 mL; withdraw the appropriate amount of the final solution to administer the intended dose.

Adults: Initially reconstitute powder with 5 mL of NS, LR, or D5W, then further dilute to a final volume of 50 mL.

For IV infusion (loading dose and continuous infusion): Prepare the 80 mg loading dose by reconstituting two 40 mg vials with NS (5 mL each); the contents of the two vials should then be further diluted in NS 100 mL. To prepare the continuous infusion, also reconstitute two 40 mg vials with NS (5 mL each); the contents of the two vials should then be further diluted in NS 100 mL.

Administration

Oral:

Capsule: Should be swallowed whole and taken at least 1 hour before eating (best if taken before breakfast). Capsule can be opened and contents mixed with 1 tablespoon of applesauce. Swallow immediately; mixture should not be chewed or warmed. For patients with difficulty swallowing, use of granules may be more appropriate.

Granules: Empty the 2.5 mg or 5 mg packet into a container with 5 mL of water or the 10 mg, 20 mg, or 40 mg packet into a container with 15 mL of water and stir; leave 2 to 3 minutes to thicken. Stir and drink within 30 minutes. If any medicine remains after drinking, add more water, stir and drink immediately.

Tablet: Swallow whole; do not crush or chew; administer with a full glass of water before breakfast in the morning.

Tablet (Canadian formulation): Swallow whole with water or may be dispersed in a half a glass of noncarbonated water. Stir until tablets disintegrate, and drink the liquid with pellets immediately or within 30 minutes. Do not chew or crush pellets. After drinking, rinse glass with water and drink.

IV: Flush line prior to and after administration with NS, LR, or D5W.

Children: Administer by intermittent infusion (10 to 30 minutes); the manufacturer recommends that children receive intravenous esomeprazole by intermittent infusion only.

Adults:

Treatment of GERD: May be administered by injection (≥3 minutes), or intermittent infusion (10 to 30 minutes)

Prevention of recurrent gastric or duodenal ulcer bleeding postendoscopy: Administer the loading dose over 30 minutes, followed by the continuous infusion at a rate of 8 mg/hour over 71.5 hours (adjust rate of continuous infusion in patients with hepatic dysfunction)

Nasogastric tube:

Capsule: Open capsule and place intact granules into a 60 mL catheter-tip syringe; mix with 50 mL of water. Replace plunger and shake vigorously for 15 seconds. Ensure that no granules remain in syringe tip. Do not administer if pellets dissolve or disintegrate. Use immediately after preparation. After administration, flush nasogastric tube with additional water.

Granules: Delayed release oral suspension granules can also be given by nasogastric or gastric tube. If using a 2.5 mg or 5 mg packet, first add 5 mL of water to a catheter-tipped syringe, then add granules from packet. If using a 10 mg, 20 mg, or 40 mg packet, first add 15 mL of water to a catheter-tipped syringe, then add granules from packet. Shake the syringe, leave 2 to 3 minutes to thicken. Shake the syringe and administer through nasogastric or gastric tube (size 6 French or greater) within 30 minutes. Refill the syringe with equal amount (5 mL or 15 mL) of water, shake and flush nasogastric/gastric tube.

Tablet (Canadian formulation): Dispersed tablets can also be given by nasogastric tube (size 8 to 20 French) using a 25 to 60 mL disposable syringe. Disperse tablet in 50 mL of water. After administration, flush with additional 25 to 50 mL of water to clear the syringe and tube. In larger nasogastric feeding tubes (ie, size 14 French or greater), the dispersion volume may be reduced to 25 mL.

Dietary Considerations

Take at least 1 hour before meals; best if taken before breakfast.

Storage

Capsules: Keep container tightly closed.

Esomeprazole magnesium: Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Esomeprazole strontium: Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Granules: Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F).

Powder for injection: Store at 25°C (77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from light. Per the manufacturer, following reconstitution, solution for injection prepared in NS, and solution for infusion prepared in NS or LR should be used within 12 hours; solution for infusion prepared in D5W should be used within 6 hours. Refrigeration is not required following reconstitution.

Additional stability data: Following reconstitution, solutions for infusion prepared in D5W, NS, or LR in PVC bags are chemically and physically stable for 48 hours at room temperature (25°C) and for at least 120 hours under refrigeration (4°C) (Kupiec, 2008).

Tablets: Store at 20°C to 25°C (68°F to 77°F).

Drug Interactions

Amphetamine: Proton Pump Inhibitors may increase the absorption of Amphetamine. Monitor therapy

Atazanavir: Proton Pump Inhibitors may decrease the serum concentration of Atazanavir. Management: See full drug interaction monograph for details. Consider therapy modification

Bisphosphonate Derivatives: Proton Pump Inhibitors may diminish the therapeutic effect of Bisphosphonate Derivatives. Monitor therapy

Bosutinib: Proton Pump Inhibitors may decrease the serum concentration of Bosutinib. Management: Consider alternatives to proton pump inhibitors, such as antacids or H2 receptor antagonists. Administer alternative agents more than 2 hours before or after bosutinib. Consider therapy modification

Cefditoren: Proton Pump Inhibitors may decrease the serum concentration of Cefditoren. Management: If possible, avoid use of cefditoren with proton pump inhibitors (PPIs). Consider alternative methods to minimize/control acid reflux (eg, diet modification) or alternative antimicrobial therapy if use of PPIs can not be avoided. Consider therapy modification

Cilostazol: CYP2C19 Inhibitors may increase the serum concentration of Cilostazol. Management: Consider reducing the cilostazol dose to 50 mg twice daily in patients who are also receiving inhibitors of CYP2C19. Consider therapy modification

Citalopram: CYP2C19 Inhibitors (Moderate) may increase the serum concentration of Citalopram. Management: Limit citalopram dose to a maximum of 20 mg/day if used with a moderate CYP2C19 inhibitor. Patients using this combination should be monitored closely for evidence of citalopram toxicity (e.g., serotonin syndrome, QT prolongation, etc.). Consider therapy modification

Clopidogrel: Esomeprazole may diminish the antiplatelet effect of Clopidogrel. Esomeprazole may decrease serum concentrations of the active metabolite(s) of Clopidogrel. Avoid combination

CYP2C19 Inducers (Strong): May increase the metabolism of CYP2C19 Substrates. Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

CYP2C19 Substrates: CYP2C19 Inhibitors (Moderate) may decrease the metabolism of CYP2C19 Substrates. Monitor therapy

Cysteamine (Systemic): Proton Pump Inhibitors may diminish the therapeutic effect of Cysteamine (Systemic). Monitor therapy

Dabigatran Etexilate: Proton Pump Inhibitors may decrease serum concentrations of the active metabolite(s) of Dabigatran Etexilate. Monitor therapy

Dabrafenib: May decrease the serum concentration of CYP2C19 Substrates. Management: Seek alternatives to the CYP2C19 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification

Dabrafenib: Proton Pump Inhibitors may decrease the serum concentration of Dabrafenib. Dabrafenib may decrease the serum concentration of Proton Pump Inhibitors. Management: Seek alternatives to the proton pump inhibitor when possible. If concomitant therapy cannot be avoided, monitor for diminished effects of both drugs. Consider therapy modification

Dasatinib: Proton Pump Inhibitors may decrease the serum concentration of Dasatinib. Management: Antacids (taken 2 hours before or after dasatinib administration) can be used in place of the proton pump inhibitor if some acid-reducing therapy is needed. Avoid combination

Delavirdine: Proton Pump Inhibitors may decrease the serum concentration of Delavirdine. Management: Chronic therapy with proton pump inhibitors (PPIs) should be avoided in patients treated with delavirdine. The clinical significance of short-term PPI therapy with delavirdine is uncertain, but such therapy should be undertaken with caution. Avoid combination

Dexmethylphenidate: Proton Pump Inhibitors may increase the absorption of Dexmethylphenidate. Specifically, proton pump inhibitors may interfere with the normal release of drug from the extended-release capsules (Focalin XR brand), which could result in both increased absorption (early) and decreased delayed absorption. Monitor therapy

Dextroamphetamine: Proton Pump Inhibitors may increase the absorption of Dextroamphetamine. Specifically, the dextroamphetamine absorption rate from mixed amphetamine salt extended release (XR) capsules may be increased in the first hours after dosing. Monitor therapy

Enzalutamide: May decrease the serum concentration of CYP2C19 Substrates. Conversely, concentrations of active metabolites may be increased for those drugs activated by CYP2C19. Management: Concurrent use of enzalutamide with CYP2C19 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP2C19 substrate should be performed with caution and close monitoring. Consider therapy modification

Erlotinib: Proton Pump Inhibitors may decrease the serum concentration of Erlotinib. Avoid combination

Fluconazole: May increase the serum concentration of Proton Pump Inhibitors. Monitor therapy

Gefitinib: Proton Pump Inhibitors may decrease the serum concentration of Gefitinib. Management: Avoid use of proton pump inhibitors (PPIs) with gefitinib when possible. If required, administer gefitinib 12 hours after administration of the PPI or 12 hours before the next dose of the PPI. Consider therapy modification

Indinavir: Proton Pump Inhibitors may decrease the serum concentration of Indinavir. Monitor therapy

Iron Salts: Proton Pump Inhibitors may decrease the absorption of Iron Salts. Exceptions: Ferric Carboxymaltose; Ferric Citrate; Ferric Gluconate; Ferric Pyrophosphate Citrate; Ferumoxytol; Iron Dextran Complex; Iron Sucrose. Monitor therapy

Itraconazole: Proton Pump Inhibitors may decrease the serum concentration of Itraconazole. Consider therapy modification

Ketoconazole (Systemic): Proton Pump Inhibitors may decrease the serum concentration of Ketoconazole (Systemic). Ketoconazole (Systemic) may increase the serum concentration of Proton Pump Inhibitors. Consider therapy modification

Ledipasvir: Proton Pump Inhibitors may decrease the serum concentration of Ledipasvir. Management: Avoid the use of PPIs at doses greater than the equivalent of omeprazole 20 mg, avoid administration of PPIs within 2 hours prior to ledipasvir dosing, and avoid use of PPIs in combination with food. Consider therapy modification

Lumacaftor: May decrease the serum concentration of CYP2C19 Substrates. Monitor therapy

Mesalamine: Proton Pump Inhibitors may diminish the therapeutic effect of Mesalamine. Proton pump inhibitor-mediated increases in gastrointestinal pH may cause the premature release of mesalamine from specific sustained-release mesalamine products. Management: Consider avoiding concurrent administration of high-dose proton pump inhibitors (PPIs) with sustained-release mesalamine products. Consider therapy modification

Methotrexate: Proton Pump Inhibitors may increase the serum concentration of Methotrexate. Monitor therapy

Methylphenidate: Proton Pump Inhibitors may increase the absorption of Methylphenidate. Specifically, proton pump inhibitors may interfere with the normal release of drug from the extended-release capsules (Ritalin LA brand), which could result in both increased absorption (early) and decreased delayed absorption. Monitor therapy

Multivitamins/Minerals (with ADEK, Folate, Iron): Proton Pump Inhibitors may decrease the serum concentration of Multivitamins/Minerals (with ADEK, Folate, Iron). Specifically, the absorption of iron may be decreased. Monitor therapy

Mycophenolate: Proton Pump Inhibitors may decrease the serum concentration of Mycophenolate. Specifically, concentrations of the active mycophenolic acid may be reduced. Monitor therapy

Nelfinavir: Proton Pump Inhibitors may decrease serum concentrations of the active metabolite(s) of Nelfinavir. Proton Pump Inhibitors may decrease the serum concentration of Nelfinavir. Avoid combination

Nilotinib: Proton Pump Inhibitors may decrease the serum concentration of Nilotinib. Management: Avoid this combination when possible since separation of doses is not likely to be an adequate method of minimizing the interaction. Consider therapy modification

PAZOPanib: Proton Pump Inhibitors may decrease the serum concentration of PAZOPanib. Avoid combination

Posaconazole: Proton Pump Inhibitors may decrease the serum concentration of Posaconazole. Consider therapy modification

Raltegravir: Proton Pump Inhibitors may increase the serum concentration of Raltegravir. Monitor therapy

RifAMPin: May decrease the serum concentration of Esomeprazole. Avoid combination

Rilpivirine: Proton Pump Inhibitors may decrease the serum concentration of Rilpivirine. Avoid combination

Riociguat: Proton Pump Inhibitors may decrease the serum concentration of Riociguat. Monitor therapy

Risedronate: Proton Pump Inhibitors may diminish the therapeutic effect of Risedronate. Proton Pump Inhibitors may increase the serum concentration of Risedronate. This applies specifically to use of delayed-release risedronate. Avoid combination

Saquinavir: Proton Pump Inhibitors may increase the serum concentration of Saquinavir. Monitor therapy

St John's Wort: May decrease the serum concentration of Esomeprazole. Avoid combination

Tacrolimus (Systemic): Proton Pump Inhibitors may increase the serum concentration of Tacrolimus (Systemic). Management: Tacrolimus dose adjustment may be required. Rabeprazole, pantoprazole, or selected H2-receptor antagonists (i.e., ranitidine or famotidine) may be less likely to interact. Genetic testing may predict patients at highest risk. Consider therapy modification

Tipranavir: May decrease the serum concentration of Proton Pump Inhibitors. These data are derived from studies with Ritonavir-boosted Tipranavir. Monitor therapy

Velpatasvir: Proton Pump Inhibitors may decrease the serum concentration of Velpatasvir. Avoid combination

Vitamin K Antagonists (eg, warfarin): Esomeprazole may increase the serum concentration of Vitamin K Antagonists. Monitor therapy

Voriconazole: May increase the serum concentration of Proton Pump Inhibitors. Proton Pump Inhibitors may increase the serum concentration of Voriconazole. Management: In patients receiving omeprazole 40 mg/day or greater, reduce omeprazole dose by half when initiating voriconazole. Monitor therapy

Test Interactions

Esomeprazole may falsely elevate serum chromogranin A (CgA) levels. The increased CgA level may cause false-positive results in the diagnosis of a neuroendocrine tumor. Temporarily stop esomeprazole ≥14 days prior to assessing CgA level; repeat level if initially elevated; use the same laboratory for all testing of CgA levels.

Adverse Reactions

Unless otherwise specified, percentages represent adverse reactions identified in clinical trials evaluating the oral formulation.

>10%: Central nervous system: Headache (IV 11%; oral 2% to 8%)

1% to 10%:

Central nervous system: Dizziness (IV 3%; oral <1%), drowsiness (adults <1%; children 2%)

Dermatologic: Pruritus (IV 1%; oral <1%)

Gastrointestinal: Flatulence (IV 10%; oral ≤5%), diarrhea (IV 4%; oral 2% to <7%), abdominal pain (IV 6%; oral 1% to 6%), nausea (IV 6%; oral 2% to 6%), xerostomia (IV 4%; oral 3%), constipation (IV 3%; oral 2%)

Local: Injection site reaction (IV 2%)

<1% (Limited to important or life-threatening): Aggression, agranulocytosis, alopecia, anaphylaxis, anemia, angioedema, anorexia, benign polyps/nodules, blurred vision, bone fracture, cervical lymphadenopathy, chest pain, chronic renal disease (Lazarus 2016), Clostridium difficile-associated diarrhea (CDAD), conjunctivitis, cyanocobalamin deficiency, cystitis, depression, dermatitis, dysgeusia, dysmenorrhea, epistaxis, erythema multiforme, exacerbation of arthritis, exacerbation of asthma, fibromyalgia syndrome, fungal infection, gastric carcinoid tumor, gastroenteritis, GI dysplasia, GI moniliasis, goiter, gynecomastia, hallucinations, hematuria, hepatic encephalopathy, hepatic failure, hepatitis, hepatotoxicity (idiosyncratic) (Chalasani, 2014), hernia, hyperhidrosis, hyperparathyroidism, hypersensitivity reactions, hypertension, hypertonia, hyperuricemia, hypoesthesia, hypokalemia, hypomagnesemia (with or without hypocalcemia and/or hypokalemia), hyponatremia, impotence, increased gastrin, increased serum alkaline phosphatase, increased serum ALT, increased serum AST, increased serum creatinine, increased thyroid-stimulating hormone, insomnia, interstitial nephritis, jaundice, laryngeal edema, leukocytosis, leukopenia, microscopic colitis, migraine, moniliasis, myasthenia, otitis media, pancreatitis, pancytopenia, parosmia, pathological fracture due to osteoporosis, phlebitis, photosensitivity, pneumonia, polymyalgia rheumatica, proteinuria, pruritus ani, rigors, skin rash (erythematous and maculopapular), Stevens-Johnson syndrome, stomatitis, tachycardia, thrombocytopenia, thrombophlebitis, ttoxic epidermal necrolysis, vaginitis, visual field defect, weight changes

Warnings/Precautions

Concerns related to adverse effects:

• Atrophic gastritis: Long-term omeprazole therapy has caused atrophic gastritis (identified by biopsy); this may also occur with esomeprazole.

• Carcinoma: No reports of enterochromaffin-like (ECL) cell carcinoids, dysplasia, or neoplasia have occurred.

Clostridium difficile-associated diarrhea (CDAD): Use of proton pump inhibitors (PPIs) may increase risk of CDAD, especially in hospitalized patients; consider CDAD diagnosis in patients with persistent diarrhea that does not improve. Use the lowest dose and shortest duration of PPI therapy appropriate for the condition being treated.

• Fractures: Increased incidence of osteoporosis-related bone fractures of the hip, spine, or wrist may occur with proton pump inhibitor (PPI) therapy. Patients on high-dose or long-term therapy should be monitored. Use the lowest effective dose for the shortest duration of time, use vitamin D and calcium supplementation, and follow appropriate guidelines to reduce risk of fractures in patients at risk.

• Gastrointestinal infection (eg, Salmonella, Campylobacter): Use of proton pump inhibitors may increase risk of these infections.

• Hypomagnesemia: Reported rarely, usually with prolonged PPI use of >3 months (most cases >1 year of therapy). May be symptomatic or asymptomatic; severe cases may cause tetany, seizures, and cardiac arrhythmias. Consider obtaining serum magnesium concentrations prior to beginning long-term therapy, especially if taking concomitant digoxin, diuretics, or other drugs known to cause hypomagnesemia; and periodically thereafter. Hypomagnesemia may be corrected by magnesium supplementation, although discontinuation of esomeprazole may be necessary; magnesium levels typically return to normal within 1 week of stopping.

• Interstitial nephritis: Acute interstitial nephritis has been observed in patients taking PPIs; may occur at any time during therapy and is generally due to an idiopathic hypersensitivity reaction. Discontinue if acute interstitial nephritis develops.

• Vitamin B12 deficiency: Prolonged treatment (≥2 years) may lead to vitamin B12 malabsorption and subsequent vitamin B12 deficiency. The magnitude of the deficiency is dose-related and the association is stronger in females and those younger in age (<30 years); prevalence is decreased after discontinuation of therapy (Lam, 2013).

Disease-related concerns:

• Gastric malignancy: Relief of symptoms does not preclude the presence of a gastric malignancy.

• Hepatic impairment: Patients with severe liver dysfunction may require dosage reductions.

• Renal impairment: Pharmacokinetics of esomeprazole are not expected to be altered in renal impairment; dosage adjustments are not necessary for any degree of renal impairment when using esomeprazole magnesium or esomeprazole sodium. However, since pharmacokinetics of the strontium may be reduced in mild to moderate renal impairment, esomeprazole strontium is not recommended for use in severe impairment (has not been studied).

Concurrent drug therapy issues:

• Clopidogrel: Proton pump inhibitors (PPIs) may diminish the therapeutic effect of clopidogrel, thought to be due to reduced formation of the active metabolite of clopidogrel. The manufacturer of clopidogrel recommends either avoidance of both omeprazole (even when scheduled 12 hours apart) and esomeprazole or use of a PPI with comparatively less effect on the active metabolite of clopidogrel (eg, pantoprazole). In contrast to these warnings, others have have recommended the continued use of PPIs, regardless of the degree of inhibition, in patients with a history of GI bleeding or multiple risk factors for GI bleeding who are also receiving clopidogrel since no evidence has established clinically meaningful differences in outcome; however, a clinically-significant interaction cannot be excluded in those who are poor metabolizers of clopidogrel (Abraham, 2010; Levine, 2011).

• Drug-drug interactions: Potentially significant interactions may exist, requiring dose or frequency adjustment, additional monitoring, and/or selection of alternative therapy. Consult drug interactions database for more detailed information.

Special populations:

• Asian ethnicity: Bioavailability may be increased in patients of Asian descent.

• Elderly: Bioavailability may be increased in the elderly.

• Pediatric: Esomeprazole strontium: Strontium competes with calcium for intestinal absorption and is incorporated into bone; use of esomeprazole strontium in pediatric patients is not recommended.

Dosage form specific issues:

• Intravenous: Safety and efficacy of IV treatment for GERD beyond 10 days have not been established; transition from IV to oral therapy as soon possible.

Other warnings/precautions:

• Appropriate use: Helicobacter pylori eradication: Short-term combination therapy (≤7 days) has been associated with a higher incidence of treatment failure. The American College of Gastroenterology recommends 10-14 days of therapy (triple or quadruple) for eradication of H. pylori (Chey, 2007).

• Laboratory test interference: Serum chromogranin A (CgA) levels increase secondary to drug-induced decreases in gastric acid; may cause false-positive results in diagnostic investigations for neuroendocrine tumors. Temporarily stop esomeprazole treatment ≥14 days before CgA test; if CgA level high, repeat test to confirm. Use same commercial laboratory for testing to prevent variable results.

• Self-medication (OTC use): When used for self-medication (OTC), notify health care provider before use if any of the following are present: heartburn for >3 months; frequent wheezing, particularly with heartburn; unexplained weight loss; nausea or vomiting; or stomach pain. Discontinue use and notify health care provider if heartburn continues or worsens; diarrhea occurs; if >14 days of therapy is needed; or if >1 course of therapy is needed every 4 months.

Monitoring Parameters

Susceptibility testing recommended in patients who fail H. pylori eradication regimen. Monitor for rebleeding in patients with peptic ulcer bleed. For patients expected to be on prolonged therapy or who take PPIs with medications such as digoxin or drugs that may cause hypomagnesemia (eg, diuretics), consider monitoring magnesium levels prior to initiation of treatment and periodically thereafter.

Pregnancy Risk Factor

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Pregnancy Considerations

Adverse events have been observed in some animal reproduction studies. An increased risk of hypospadias was reported following maternal use of proton pump inhibitors (PPIs) during pregnancy (Anderka, 2012), but this was based on a small number of exposures and the same association was not found in another study (Erichsen, 2012). An increased risk of major birth defects following maternal use of PPIs during pregnancy was not observed in an additional study (Pasternak, 2010). Esomeprazole is the s-isomer of omeprazole; refer to the omeprazole monograph for additional information. When treating GERD in pregnancy, PPIs may be used when clinically indicated (Katz, 2013).

Patient Education

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience headache, fatigue, constipation, flatulence, nausea, or dry mouth. Have patient report immediately to prescriber signs of low magnesium (mood changes; muscle pain or weakness; muscle cramps or spasms; seizures; tremors; lack of appetite; severe nausea or vomiting; or an abnormal heartbeat), signs of kidney problems (urinary retention, blood in urine, change in amount of urine passed, or weight gain), severe dizziness, passing out, severe abdominal pain, bone pain, chills, pharyngitis, shortness of breath, excessive weight loss, severe diarrhea, bloody stools, signs of Stevens-Johnson syndrome/toxic epidermal necrolysis (red, swollen, blistered, or peeling skin [with or without fever]; red or irritated eyes; or sores in mouth, throat, nose, or eyes), or injection site irritation (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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