esomeprazole (Rx, OTC)

Brand and Other Names:Nexium, Nexium 24HR

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule, delayed-release (as magnesium)

  • 20mg (Rx/OTC)
  • 40mg
  • 24.65mg (strontium salt)
  • 49.3mg (strontium salt)

tablet delayed release (as magnesium)

  • 20 mg

injection, powder for reconstitution

  • 20mg/vial
  • 40mg/vial

packets for oral suspension

  • 10mg
  • 20mg
  • 40mg

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

Eosinophilic Esophagitis (Orphan)

Orphan designation for treatment of eosinophilic esophagitis

Orphan sponsor

  • Adare Pharmaceuticals, Inc; 845 Center Drive; Vandalia, Ohio 45377

Dosage Forms & Strengths

capsule, delayed-release

  • 20mg
  • 40mg

tablet delayed release

  • 20mg

injection, powder for reconstitution

  • 20mg/vial
  • 40mg/vial

packets for oral suspension

  • 10mg
  • 20mg
  • 40mg

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
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Interactions

Interaction Checker

and esomeprazole

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        Significant - Monitor Closely

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            Contraindicated (4)

            • erlotinib

              esomeprazole decreases levels of erlotinib by Other (see comment). Contraindicated. Comment: Concomitant use of proton pump inhibitors with erlotinib should be avoided if possible. Drugs that alter pH of upper GI tract may alter the solubility of erlotinib and reduce its bioavailability. .

            • mavacamten

              esomeprazole will increase the level or effect of mavacamten by affecting hepatic enzyme CYP2C19 metabolism. Contraindicated. Strong or moderate CYP2C19 inhibitors may increase mavacamten systemic exposure, resulting in heart failure due to systolic dysfunction.

            • nelfinavir

              esomeprazole decreases levels of nelfinavir by unspecified interaction mechanism. Contraindicated. Coadministration may lead to loss of nelfinavir virologic response and development of resistance; mechanism may be CYP2C19 inhibition of nelfinavir conversion to active M8 metabolite, and also PPIs decreasing gastric pH resulting in decreased nelfinavir absorption.

            • rilpivirine

              esomeprazole decreases levels of rilpivirine by increasing gastric pH. Applies only to oral form of both agents. Contraindicated. Concurrent use may cause treatment failure and/or the development of rilpivirine or NNRTI resistance owing to decreased levels.

            Serious - Use Alternative (35)

            • acalabrutinib

              esomeprazole decreases levels of acalabrutinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Acalabrutinib solubility decreases with increasing gastric pH. Due to the long-lasting effect of PPIs, separation of doses may not eliminate the interaction.

            • apalutamide

              apalutamide will decrease the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP2C19 inducer, with drugs that are CYP2C19 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered.

              apalutamide will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Coadministration of apalutamide, a strong CYP3A4 inducer, with drugs that are CYP3A4 substrates can result in lower exposure to these medications. Avoid or substitute another drug for these medications when possible. Evaluate for loss of therapeutic effect if medication must be coadministered. Adjust dose according to prescribing information if needed.

            • atazanavir

              esomeprazole will decrease the level or effect of atazanavir by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Atazanavir solubility decreases as pH increases. Substantially reduced plasma concentrations of atazanavir are expected if PPIs are coadministered. PPI dose should not exceed a dose comparable to omeprazole 20 mg and must be taken ~12 h before atazanavir/ritonavir in treatment naive-patients. PPIs are not recommended in treatment-experienced taking atazanavir.

            • carbamazepine

              carbamazepine will decrease the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug.

            • ceritinib

              esomeprazole will decrease the level or effect of ceritinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • cilostazol

              esomeprazole increases toxicity of cilostazol by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Decrease cilostazol dose by 50%; 3,4-dehydrocilostazol, an active metabolite, increased by 69% as a result of omeprazole inhibition of CYP2C19.

            • clopidogrel

              esomeprazole decreases effects of clopidogrel by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Clopidogrel efficacy may be reduced by drugs that inhibit CYP2C19. Inhibition of platelet aggregation by clopidogrel is entirely due to an active metabolite. Clopidogrel is metabolized to this active metabolite in part by CYP2C19. .

            • dacomitinib

              esomeprazole will increase the level or effect of dacomitinib by unspecified interaction mechanism. Avoid or Use Alternate Drug. Concomitant use with a PPI decreases dacomitinib concentrations, which may reduce dacomitinib efficacy. Avoid use of PPIs with dacomitinib. As an alternative to PPIs, use locally-acting antacids or an H2-receptor antagonist. Administer at least 6 hours before or 10 hours after taking an H2-receptor antagonist.

            • dasatinib

              esomeprazole will decrease the level or effect of dasatinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • digoxin

              esomeprazole will increase the level or effect of digoxin by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • enzalutamide

              enzalutamide will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • fexinidazole

              fexinidazole will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Fexinidazole inhibits CYP3A4. Coadministration may increase risk for adverse effects of CYP3A4 substrates.

            • fluvoxamine

              fluvoxamine will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug.

            • idelalisib

              idelalisib will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Idelalisib is a strong CYP3A inhibitor; avoid coadministration with sensitive CYP3A substrates

            • indinavir

              esomeprazole will decrease the level or effect of indinavir by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • infigratinib

              esomeprazole will decrease the level or effect of infigratinib by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • isoniazid

              isoniazid will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug.

            • itraconazole

              esomeprazole will decrease the level or effect of itraconazole by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • ketoconazole

              esomeprazole will decrease the level or effect of ketoconazole by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • levoketoconazole

              esomeprazole will decrease the level or effect of levoketoconazole by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • lonafarnib

              lonafarnib will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Avoid or Use Alternate Drug. Lonafarnib may increase the AUC and peak concentration of CYP2C19 substrates. If coadministration unavoidable, monitor for adverse reactions and reduce the CYP2C19 substrate dose in accordance with its approved product labeling.

            • mesalamine

              esomeprazole decreases effects of mesalamine by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Applies only to sustained release dosage form.

            • neratinib

              esomeprazole will decrease the level or effect of neratinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • nilotinib

              esomeprazole will decrease the level or effect of nilotinib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Nilotinib has a pH-dependent solubility and solubility is decreased at higher pH; separating doses may not eliminate this effect because of PPI extended duration of action

            • nisoldipine

              esomeprazole will increase the level or effect of nisoldipine by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug.

            • pazopanib

              esomeprazole will decrease the level or effect of pazopanib by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Avoid coadministration of pazopanib with drugs that raise gastric pH; consider short-acting antacids in place of PPIs and H2 antagonists; separate antacid and pazopanib dosing by several hours

            • pexidartinib

              esomeprazole will decrease the level or effect of pexidartinib by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Avoid coadministration of proton pump inhibitors (PPIs) with pexidartinib. Use H2-receptor antagonists or antacids if needed. When using alternatives to PPIs, administer pexidartinib 2 hr before or after taking locally-acting antacids OR administer pexidartinib at least 2 hr before or 10 hr after taking an H2-receptor antagonist.

            • phenobarbital

              phenobarbital will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • secobarbital

              secobarbital will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug.

            • secretin

              esomeprazole, secretin. Other (see comment). Avoid or Use Alternate Drug. Comment: Concomitant use of PPIs may cause a hyperresponse in gastrin secretion in response to stimulation testing with secretin, falsely suggesting gastrinoma. The time it takes for serum gastrin concentrations to return to baseline following discontinuation of PPIs is specific to the individual PPI. Temporarily stop esomeprazole treatment at least 14 days before assessing to allow gastrin levels to return to baseline.

            • sofosbuvir/velpatasvir

              esomeprazole will decrease the level or effect of sofosbuvir/velpatasvir by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Velpatasvir solubility decreases as gastric pH increases (practically insoluble at pH >5). Coadministration of sofosbuvir/velpatasvir with omeprazole or other PPIs is not recommended. If considered medically necessary, give sofosbuvir/velpatasvir with food 4 hr before omeprazole 20 mg. Use with other PPIs has not been studied.

            • sotorasib

              esomeprazole will decrease the level or effect of sotorasib by inhibition of GI absorption. Applies only to oral form of both agents. Avoid or Use Alternate Drug. If use with an acid-reducing agent cannot be avoided, administer sotorasib 4 hr before or 10 hr after administration of a locally-acting antacid.

            • sparsentan

              esomeprazole decreases effects of sparsentan by increasing gastric pH. Applies only to oral form of both agents. Avoid or Use Alternate Drug. Proton pump inhibitors may decrease sparsentan exposure which may reduce efficacy of sparsentan.

            • tucatinib

              tucatinib will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Avoid concomitant use of tucatinib with CYP3A substrates, where minimal concentration changes may lead to serious or life-threatening toxicities. If unavoidable, reduce CYP3A substrate dose according to product labeling.

            • voxelotor

              voxelotor will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. Voxelotor increases systemic exposure of sensitive CYP3A4 substrates. Avoid coadministration with sensitive CYP3A4 substrates with a narrow therapeutic index. Consider dose reduction of the sensitive CYP3A4 substrate(s) if unable to avoid.

            Monitor Closely (84)

            • amitriptyline

              esomeprazole will increase the level or effect of amitriptyline by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • amobarbital

              amobarbital will decrease the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              amobarbital will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • ampicillin

              esomeprazole will decrease the level or effect of ampicillin by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • armodafinil

              armodafinil will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • axitinib

              esomeprazole will increase the level or effect of axitinib by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • belumosudil

              esomeprazole will decrease the level or effect of belumosudil by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Increase belumosudil dosage to 200 mg PO BID when coadministered with proton pump inhibitors.

            • belzutifan

              belzutifan will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. If unable to avoid coadministration of belzutifan with sensitive CYP3A4 substrates, consider increasing the sensitive CYP3A4 substrate dose in accordance with its prescribing information.

            • bendamustine

              esomeprazole decreases levels of bendamustine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor. Consentration of active metabolites may be increased.

            • bortezomib

              bortezomib will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • bosentan

              bosentan will decrease the level or effect of esomeprazole by increasing metabolism. Use Caution/Monitor.

              bosentan will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • bosutinib

              esomeprazole will decrease the level or effect of bosutinib by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Bosutinib displays pH dependent solubility

            • budesonide

              esomeprazole decreases effects of budesonide by increasing gastric pH. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Enteric-coated budesonide dissolves at pH >5.5. Also, dissolution of extended-release budesonide tablets is pH dependent. Coadministration with drugs that increase gastric pH may cause these budesonide products to prematurely dissolve, and possibly affect release properties and absorption of the drug in the duodenum.

            • butabarbital

              butabarbital will decrease the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • cannabidiol

              esomeprazole will increase the level or effect of cannabidiol by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider reducing the cannabidiol dose when coadministered with a moderate CYP2C19 inhibitor.

              cannabidiol will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider reducing the dose of sensitive CYP2C19 substrates, as clinically appropriate, when coadministered with cannabidiol.

            • carbamazepine

              carbamazepine will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • carbonyl iron

              esomeprazole will decrease the level or effect of carbonyl iron by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • cefpodoxime

              esomeprazole will decrease the level or effect of cefpodoxime by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • cefuroxime

              esomeprazole will decrease the level or effect of cefuroxime by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • cenobamate

              cenobamate will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Increase dose of CYP3A4 substrate, as needed, when coadministered with cenobamate.

              cenobamate will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider a dose reduction of CYP2C19 substrates, as clinically appropriate, when used concomitantly with cenobamate.

            • citalopram

              esomeprazole will increase the level or effect of citalopram by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Citalopram 20 mg/day is the maximum recommended dose for patients taking CYP2C19 inhibitors because of the risk of QT prolongation.

            • clobazam

              esomeprazole will increase the level or effect of clobazam by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Dosage adjustment may be required; CYP2C19 inhibitors may result in increased exposure to N-desmethylclobazam (active metabolite).

            • clozapine

              esomeprazole will decrease the level or effect of clozapine by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • cobicistat

              cobicistat will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • crizotinib

              esomeprazole decreases levels of crizotinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Drugs that elevate the gastric pH may decrease the solubility of crizotinib and subsequently reduce its bioavailability. However, no formal studies have been conducted. .

            • crofelemer

              crofelemer increases levels of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Crofelemer has the potential to inhibit CYP3A4 at concentrations expected in the gut; unlikely to inhibit systemically because minimally absorbed.

            • cyclosporine

              cyclosporine, esomeprazole. Either increases toxicity of the other by Other (see comment). Use Caution/Monitor. Comment: When used for prolonged periods of time PPIs may cause hypomagnesemia and the risk is further increased when used concomitantly with drugs that also have the same effects.

            • dabrafenib

              esomeprazole will decrease the level or effect of dabrafenib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Drugs that alter upper GI tract pH (eg, PPIs, H2-blockers, antacids) may decrease dabrafenib solubility and reduce its bioavailability

              dabrafenib will decrease the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Use alternative if available

            • dextroamphetamine

              esomeprazole, dextroamphetamine. Other (see comment). Use Caution/Monitor. Comment: Reduced gastric acidity caused by proton pump inhibitors decreases time to Tmax for amphetamine and dextroamphetamine. AUC was unaffected. .

            • diazepam intranasal

              esomeprazole will increase the level or effect of diazepam intranasal by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Strong or moderate CYP2C19 inhibitors may decrease rate of diazepam elimination, thereby increasing adverse reactions to diazepam.

            • dichlorphenamide

              dichlorphenamide and esomeprazole both decrease serum potassium. Use Caution/Monitor.

            • digoxin

              esomeprazole increases toxicity of digoxin by Other (see comment). Use Caution/Monitor. Comment: Prolonged use of PPIs may cause hypomagnesemia and increase risk for digoxin toxicity.

            • duloxetine

              esomeprazole will decrease the level or effect of duloxetine by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • efavirenz

              efavirenz will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • elagolix

              elagolix will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak CYP2C19 inhibitor. Caution with sensitive CYP2C19 substrates.

              elagolix will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Modify Therapy/Monitor Closely. Elagolix is a weak-to-moderate CYP3A4 inducer. Monitor CYP3A substrates if coadministered. Consider increasing CYP3A substrate dose if needed.

            • eltrombopag

              esomeprazole will decrease the level or effect of eltrombopag by affecting hepatic enzyme CYP1A2 metabolism. Use Caution/Monitor.

            • escitalopram

              esomeprazole will increase the level or effect of escitalopram by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • eslicarbazepine acetate

              eslicarbazepine acetate will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • etravirine

              esomeprazole will increase the level or effect of etravirine by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              etravirine will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • fedratinib

              fedratinib will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP3A4 substrates as necessary.

              fedratinib will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Adjust dose of drugs that are CYP2C19 substrates as necessary.

            • ferric gluconate

              esomeprazole will decrease the level or effect of ferric gluconate by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • ferric maltol

              esomeprazole will decrease the level or effect of ferric maltol by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • ferrous fumarate

              esomeprazole will decrease the level or effect of ferrous fumarate by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • ferrous gluconate

              esomeprazole will decrease the level or effect of ferrous gluconate by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • ferrous sulfate

              esomeprazole will decrease the level or effect of ferrous sulfate by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • fexinidazole

              fexinidazole will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • fluconazole

              fluconazole will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • fosamprenavir

              esomeprazole will decrease the level or effect of fosamprenavir by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • fosphenytoin

              esomeprazole will increase the level or effect of fosphenytoin by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              fosphenytoin will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • gefitinib

              esomeprazole decreases levels of gefitinib by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Avoid coadministration of gefitinib with PPIs if possible. If treatment with a PPI is required, separate gefitinib and PPI doses by 12 hr.

            • glipizide

              esomeprazole will increase the level or effect of glipizide by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • glyburide

              esomeprazole will increase the level or effect of glyburide by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • iloperidone

              iloperidone increases levels of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Iloperidone is a time-dependent CYP3A inhibitor and may lead to increased plasma levels of drugs predominantly eliminated by CYP3A4.

            • imipramine

              esomeprazole will increase the level or effect of imipramine by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • iron dextran complex

              esomeprazole will decrease the level or effect of iron dextran complex by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • iron sucrose

              esomeprazole will decrease the level or effect of iron sucrose by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • istradefylline

              istradefylline will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Istradefylline 40 mg/day increased peak levels and AUC of CYP3A4 substrates in clinical trials. This effect was not observed with istradefylline 20 mg/day. Consider dose reduction of sensitive CYP3A4 substrates.

            • ledipasvir/sofosbuvir

              esomeprazole decreases levels of ledipasvir/sofosbuvir by Other (see comment). Use Caution/Monitor. Comment: Ledipasvir solubility decreases as pH increases; drugs that increase gastric pH are expected to decrease levels of ledipasvir; proton-pump inhibitor doses comparable to omeprazole <20 mg can be administered simultaneously with ledipasvir/sofosbuvir under fasted conditions.

            • lenacapavir

              lenacapavir will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lencapavir (a moderate CYP3A4 inhibitor) may increase CYP3A4 substrates initiated within 9 months after last SC dose of lenacapavir, which may increase potential risk of adverse reactions of CYP3A4 substrates.

            • letermovir

              letermovir increases levels of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • lumacaftor/ivacaftor

              lumacaftor/ivacaftor, esomeprazole. affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. In vitro studies suggest that lumacaftor may induce and ivacaftor may inhibit CYP2C19 substrates. .

              lumacaftor/ivacaftor will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Lumacaftor/ivacaftor is a strong CYP3A4 inhibitor and also has the potential to induce CYP2C19 and both induce and inhibitor P-gp.

            • methotrexate

              esomeprazole increases levels of methotrexate by decreasing renal clearance. Use Caution/Monitor. Increased risk of toxicity with higher doses.

            • methylphenidate

              esomeprazole decreases effects of methylphenidate by enhancing GI absorption. Applies only to oral form of both agents. Modify Therapy/Monitor Closely. Since the characteristics of methylphenidate extended release capsules (Ritalin LA) are pH dependent, coadministration of antacids or acid suppressants could alter the release of methylphenidate. Consider separating the administration of the antacid and the methylphenidate extended-release capsules may be avoided.

            • mitotane

              mitotane decreases levels of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor. Mitotane is a strong inducer of cytochrome P-4503A4; monitor when coadministered with CYP3A4 substrates for possible dosage adjustments.

            • mycophenolate

              esomeprazole will decrease the level or effect of mycophenolate by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor. Potential interaction applies to mycophenolate mofetil. Enteric coated mycophenolate sodium formulation is less sensitive to this interaction. Clinical significance unclear.

            • pentobarbital

              pentobarbital will decrease the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • phenobarbital

              phenobarbital will decrease the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • phenytoin

              esomeprazole will increase the level or effect of phenytoin by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              phenytoin will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • polysaccharide iron

              esomeprazole will decrease the level or effect of polysaccharide iron by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • posaconazole

              esomeprazole will decrease the level or effect of posaconazole by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

              posaconazole will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • primidone

              primidone will decrease the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • rifampin

              rifampin will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

              rifampin will decrease the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • riociguat

              esomeprazole will decrease the level or effect of riociguat by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • ritonavir

              ritonavir will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • rose hips

              esomeprazole will decrease the level or effect of rose hips by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • secobarbital

              secobarbital will decrease the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

            • sparsentan

              sparsentan will decrease the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Sparsentan (a CYP2C19 inducer) decreases exposure of CYP2C19 substrates and reduces efficacy related to these substrates.

            • St John's Wort

              St John's Wort will decrease the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              St John's Wort will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • stiripentol

              stiripentol will decrease the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Modify Therapy/Monitor Closely. Consider reducing the dose of CYP2C19 substrates, if adverse reactions are experienced when administered concomitantly with stiripentol.

            • tacrolimus

              esomeprazole will increase the level or effect of tacrolimus by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. Concomitant administration may increase tacrolimus whole blood concentrations, particularly in intermediate or poor metabolizers of CYP2C19

            • tazemetostat

              tazemetostat will decrease the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            • tolbutamide

              esomeprazole will increase the level or effect of tolbutamide by increasing gastric pH. Applies only to oral form of both agents. Use Caution/Monitor.

            • triclabendazole

              triclabendazole will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor. If plasma concentrations of the CYP2C19 substrates are elevated during triclabendazole, recheck plasma concentration of the CYP2C19 substrates after discontinuation of triclabendazole.

            • vismodegib

              esomeprazole will decrease the level or effect of vismodegib by Other (see comment). Use Caution/Monitor. Drugs that increase gastric pH alter vismodegib solubility and therefore reduce bioavailability; effect on efficacy unknown

            • voriconazole

              voriconazole will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Use Caution/Monitor.

              voriconazole will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Use Caution/Monitor.

            Minor (44)

            • acetazolamide

              acetazolamide will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • alosetron

              esomeprazole will decrease the level or effect of alosetron by increasing metabolism. Minor/Significance Unknown.

            • alprazolam

              esomeprazole increases levels of alprazolam by decreasing metabolism. Minor/Significance Unknown.

            • ambrisentan

              esomeprazole will increase the level or effect of ambrisentan by affecting hepatic enzyme CYP2C19 metabolism. Minor/Significance Unknown.

            • anastrozole

              anastrozole will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • bismuth subsalicylate

              esomeprazole increases levels of bismuth subsalicylate by enhancing GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

            • blessed thistle

              blessed thistle decreases effects of esomeprazole by pharmacodynamic antagonism. Minor/Significance Unknown. Theoretical interaction.

            • bosentan

              esomeprazole will increase the level or effect of bosentan by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

            • capecitabine

              esomeprazole decreases effects of capecitabine by unknown mechanism. Minor/Significance Unknown. Retrospective data suggest elevated gastric pH caused by PPI use may impair capecitabine tablet dissolution and/or reduce absorption. However, a randomized crossover study found esomeprazole did not affect capecitabine systemic exposure.

            • chlordiazepoxide

              esomeprazole will increase the level or effect of chlordiazepoxide by decreasing metabolism. Minor/Significance Unknown.

            • clomipramine

              esomeprazole will increase the level or effect of clomipramine by affecting hepatic enzyme CYP2C19 metabolism. Minor/Significance Unknown.

            • clonazepam

              esomeprazole will increase the level or effect of clonazepam by affecting hepatic enzyme CYP2C19 metabolism. Minor/Significance Unknown.

            • cyanocobalamin

              esomeprazole decreases levels of cyanocobalamin by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

            • cyclophosphamide

              cyclophosphamide will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • darifenacin

              darifenacin will decrease the level or effect of esomeprazole by Other (see comment). Minor/Significance Unknown. Effectiveness of proton pump inhibitors may be decreased theoretically if administered with other antisecretory agents

            • devil's claw

              devil's claw decreases effects of esomeprazole by pharmacodynamic antagonism. Minor/Significance Unknown.

            • dexamethasone

              dexamethasone will decrease the level or effect of esomeprazole by increasing metabolism. Minor/Significance Unknown.

            • diazepam

              esomeprazole will increase the level or effect of diazepam by affecting hepatic enzyme CYP2C19 metabolism. Minor/Significance Unknown.

            • dronedarone

              dronedarone will increase the level or effect of esomeprazole by decreasing metabolism. Minor/Significance Unknown.

            • efavirenz

              efavirenz will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Minor/Significance Unknown.

            • elvitegravir/cobicistat/emtricitabine/tenofovir DF

              elvitegravir/cobicistat/emtricitabine/tenofovir DF, esomeprazole. affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown. Based on drug interaction studies conducted with the components of Stribild, no clinically significant drug interactions have been either observed or are expected when coadministered with PPIs.

            • eslicarbazepine acetate

              eslicarbazepine acetate decreases levels of esomeprazole by increasing metabolism. Minor/Significance Unknown. Monitor for GI symptoms; net increased or decreased effect on PPI action unclear due to opposing CYP450 actions.

            • estazolam

              esomeprazole will increase the level or effect of estazolam by affecting hepatic enzyme CYP2C19 metabolism. Minor/Significance Unknown.

            • ferric carboxymaltose

              esomeprazole will decrease the level or effect of ferric carboxymaltose by increasing gastric pH. Applies only to oral form of both agents. Minor/Significance Unknown.

            • fluoxetine

              fluoxetine will increase the level or effect of esomeprazole by affecting hepatic enzyme CYP2C19 metabolism. Minor/Significance Unknown.

            • flurazepam

              esomeprazole increases levels of flurazepam by decreasing metabolism. Minor/Significance Unknown.

            • fluvastatin

              esomeprazole will increase the level or effect of fluvastatin by affecting hepatic enzyme CYP2C9/10 metabolism. Minor/Significance Unknown.

            • itraconazole

              itraconazole will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • larotrectinib

              larotrectinib will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • levoketoconazole

              levoketoconazole will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • levothyroxine

              esomeprazole decreases levels of levothyroxine by increasing gastric pH. Applies only to oral form of both agents. Minor/Significance Unknown. Conflicting evidence regarding this interaction exists.

            • liothyronine

              esomeprazole decreases levels of liothyronine by increasing gastric pH. Applies only to oral form of both agents. Minor/Significance Unknown. Conflicting evidence regarding this interaction exists.

            • liotrix

              esomeprazole decreases levels of liotrix by increasing gastric pH. Applies only to oral form of both agents. Minor/Significance Unknown. Conflicting evidence regarding this interaction exists.

            • lisdexamfetamine

              esomeprazole, lisdexamfetamine. Other (see comment). Minor/Significance Unknown. Comment: Reduced gastric acidity caused by proton pump inhibitors decreases time to Tmax for amphetamine and dextroamphetamine. AUC was unaffected. .

            • lorazepam

              esomeprazole increases levels of lorazepam by decreasing metabolism. Minor/Significance Unknown.

            • methamphetamine

              esomeprazole decreases levels of methamphetamine by Other (see comment). Minor/Significance Unknown. Comment: Time to maximum concentration (Tmax) of amphetamine is decreased compared to when administered alone; monitor patients for changes in clinical effect and adjust therapy based on clinical response.

            • midazolam

              esomeprazole increases levels of midazolam by decreasing metabolism. Minor/Significance Unknown.

            • phytoestrogens

              esomeprazole decreases levels of phytoestrogens by inhibition of GI absorption. Applies only to oral form of both agents. Minor/Significance Unknown.

            • ponatinib

              esomeprazole decreases levels of ponatinib by increasing gastric pH. Applies only to oral form of both agents. Minor/Significance Unknown.

            • ribociclib

              ribociclib will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Minor/Significance Unknown.

            • theophylline

              esomeprazole increases toxicity of theophylline by Other (see comment). Minor/Significance Unknown. Comment: Prolonged use of proton pump inhibitors can cause hypochlorhydria, which in turn causes peristalsis in small intestine to increase and peristalsis in the proximal colon to decrease; monitor for toxicity.

            • thyroid desiccated

              esomeprazole decreases levels of thyroid desiccated by increasing gastric pH. Applies only to oral form of both agents. Minor/Significance Unknown. Conflicting evidence regarding this interaction exists.

            • triazolam

              esomeprazole increases levels of triazolam by affecting hepatic enzyme CYP2C19 metabolism. Minor/Significance Unknown.

            • voriconazole

              esomeprazole will increase the level or effect of voriconazole by affecting hepatic enzyme CYP2C19 metabolism. Minor/Significance Unknown.

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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)

            Postmarketing Reports

            Cutaneous and systemic lupus erythematosus

            Cyanocobalamin (vitamin B-12) deficiency

            Clostridium difficile-associated diarrhea

            Fundic gland polyps

            Acute tubulointerstitial nephritis

            Hypocalcemia

            Drug reaction with eosinophilia and systemic symptoms (DRESS), acute generalized exanthematous pustulosis (AGEP)

            Erectile dysfunction

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            Warnings

            Contraindications

            Hypersensitivity to esomeprazole or other proton pump inhibitors (PPIs)

            Patients receiving rilpivirine- containing products

            Cautions

            Do not use if allergic to the drug; may cause severe skin reactions; symptoms may include, skin reddening, blisters, rash; if allergic reaction occurs, discontinue use and seek medical help immediately

            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

            Severe hepatic impairment

            Cutaneous lupus erythematosus (CLE) and systemic lupus erythematosus (SLE) reported with PPIs; avoid using for longer than medically indicated; discontinue if signs or symptoms consistent with CLE or SLE are observed and refer patient to specialist; most patients improve with discontinuation of PPI alone in 4-12 weeks; serological testing (e.g. ANA) may be positive and elevated serological test results may take longer to resolve than clinical manifestations

            Severe cutaneous adverse reactions, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN), drug reaction with eosinophilia and systemic symptoms (DRESS), and acute generalized exanthematous pustulosis (AGEP) reported in association with use of PPIs; discontinue therapy at first signs or symptoms of severe cutaneous adverse reactions or other signs of hypersensitivity and consider further evaluation

            Relief of symptoms does not eliminate the possibility of a gastric malignancy; consider additional follow-up and diagnostic testing in adult patients who have suboptimal response or early symptomatic relapse after completing treatment with a PPI

            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

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

            If patient taking a prescription drug, the patient should ask a doctor or a pharmacist whether acid reducers can be taken concomitantly with it

            Acute interstitial nephritis reported in patients taking proton pump inhibitors

            May elevate and/or prolong serum concentrations of methotrexate and/or its metabolite when administered concomitantly with PPIs, possibly leading to toxicity; consider a temporary withdrawal of PPI therapy with high dose methotrexate administration

            Stop use and inform a healthcare professional if rash or joint pain develops

            PPI therapy is associated with increased risk of fundic gland polyp; risk increases with long-term use >1 year; patient may be asymptomatic; problem usually identified incidentally on endoscopy; use shortest duration of therapy appropriate to condition being treated

            Acute tubulointerstitial nephritis (TIN) reported in patients taking PPIs; may occur at any point during PPI therapy; patients may present with varying signs and symptoms from symptomatic hypersensitivity reactions to non-specific symptoms of decreased renal function (e.g., malaise, nausea, anorexia); in reported case series, some patients were diagnosed on biopsy and in absence of extra-renal manifestations (eg, fever, rash or arthralgia); discontinue therapy and evaluate patients with suspected acute TIN

            Hypomagnesemia and mineral metabolism

            • 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; consider monitoring magnesium levels prior to initiation of PPI treatment and periodically
            • Hypomagnesemia may lead to hypocalcemia and/or hypokalemia and may exacerbate underlying hypocalcemia in at-risk patients; in most patients, treatment of hypomagnesemia required magnesium replacement and discontinuation of the PPI
            • Consider monitoring magnesium and calcium levels prior to initiation of therapy and periodically while on treatment in patients with a preexisting risk of hypocalcemia (eg, hypoparathyroidism); supplement with magnesium and/or calcium as necessary. If hypocalcemia is refractory to treatment, consider discontinuing the PPI
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            Pregnancy & Lactation

            Pregnancy

            There are no adequate and well-controlled studies 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)

            Lactation

            Esomeprazole is the S-isomer of omeprazole and limited data suggest that omeprazole may be present in human milk; there are no clinical data on effects of esomeprazole on breastfed infant or on milk production; developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed infant from treatment or from underlying maternal condition

            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.

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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

            Oral Administration

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

            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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            Nexium 24HR oral
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            20 mg capsule
            Nexium 24HR oral
            -
            20 mg tablet

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            Patient Handout

            A Patient Handout is not currently available for this monograph.
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            Formulary

            FormularyPatient Discounts

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            Tier Description
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.