Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
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 (36)
- abametapir
abametapir will increase the level or effect of esomeprazole by affecting hepatic/intestinal enzyme CYP3A4 metabolism. Avoid or Use Alternate Drug. For 2 weeks after abametapir application, avoid taking drugs that are CYP3A4 substrates. If not feasible, avoid use of abametapir.
- 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.
- ponatinib
esomeprazole decreases levels of ponatinib by increasing gastric pH. Applies only to oral form of both agents. 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.
- 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 (82)
- 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.
- 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.
- 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 (38)
- 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.
- 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.
- 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.
- 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.
- 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.
- 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.
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)
Warnings
Contraindications
Hypersensitivity to esomeprazole or other proton pump inhibitors (PPIs)
Patients receiving rilpivirine- containing products
Cautions
PPIs are possibly associated with increased incidence of Clostridium difficile-associated diarrhea (CDAD); consider diagnosis of CDAD for patients taking PPIs who have diarrhea that does not improve
PPIs may decrease the efficacy of clopidogrel by reducing the formation of the active metabolite
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
Breastfeeding
Therapy increases risk of Salmonella, Campylobacter, and other infections
Contains enteric coated granules (acid labile); do not chew or crush; take 1 hr before meals
Published observational studies suggest that PPI therapy may be associated with an increased risk for osteoporosis-related fractures of the hip, wrist, or spine; particularly with prolonged (>1 yr), high-dose therapy
Decreased gastric acidity increases serum chromogranin A (CgA) levels and may cause false-positive diagnostic results for neuroendocrine tumors; temporarily discontinue PPIs before assessing CgA levels
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
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.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
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
Images
| BRAND | FORM. | UNIT PRICE | PILL IMAGE |
|---|---|---|---|
| Nexium 24HR oral - | 20 mg capsule |  | |
| Nexium 24HR oral - | 20 mg tablet |  | |
| Nexium oral - | 20 mg capsule |  | |
| Nexium oral - | 40 mg capsule |  | |
| Nexium oral - | 40 mg capsule |  | |
| esomeprazole magnesium oral - | 40 mg capsule |  | |
| esomeprazole magnesium oral - | 40 mg capsule |  | |
| esomeprazole magnesium oral - | 20 mg capsule |  | |
| esomeprazole magnesium oral - | 20 mg capsule |  | |
| esomeprazole magnesium oral - | 20 mg capsule |  | |
| esomeprazole magnesium oral - | 40 mg capsule |  | |
| esomeprazole magnesium oral - | 40 mg capsule |  | |
| esomeprazole magnesium oral - | 40 mg capsule |  | |
| esomeprazole magnesium oral - | 40 mg capsule |  | |
| esomeprazole magnesium oral - | 20 mg capsule |  | |
| esomeprazole magnesium oral - | 20 mg capsule |  | |
| esomeprazole magnesium oral - | 40 mg capsule |  | |
| esomeprazole magnesium oral - | 20 mg capsule |  | |
| esomeprazole magnesium oral - | 20 mg capsule |  | |
| esomeprazole magnesium oral - | 40 mg capsule |  | |
| esomeprazole magnesium oral - | 20 mg capsule |  | |
| esomeprazole magnesium oral - | 40 mg capsule |  | |
| esomeprazole magnesium oral - | 20 mg capsule |  | |
| esomeprazole magnesium oral - | 20 mg capsule |  | |
| esomeprazole magnesium oral - | 20 mg capsule |  | |
| esomeprazole magnesium oral - | 20 mg capsule |  | |
| Nexium Packet oral - | 40 mg powder |  | |
| Nexium Packet oral - | 2.5 mg powder |  | |
| Nexium Packet oral - | 5 mg powder |  | |
| Nexium Packet oral - | 20 mg powder |  | |
| Nexium Packet oral - | 10 mg powder |  |
Copyright © 2010 First DataBank, Inc.
Patient Handout
esomeprazole magnesium oral
ESOMEPRAZOLE DELAYED-RELEASE TABLET - ORAL
(ES-oh-MEP-ra-zole)
COMMON BRAND NAME(S): Nexium 24HR
USES: Esomeprazole is used to treat certain stomach and esophagus problems (such as acid reflux, ulcers). It works by decreasing the amount of acid your stomach makes. It relieves symptoms such as heartburn, difficulty swallowing, and cough. This medication helps heal acid damage to the stomach and esophagus, helps prevent ulcers, and may help prevent cancer of the esophagus. Esomeprazole belongs to a class of drugs known as proton pump inhibitors (PPIs).If you are self-treating with this medication, over-the-counter esomeprazole products are used to treat frequent heartburn (occurring 2 or more days a week). Since it may take 1 to 4 days to have full effect, these products do not relieve heartburn right away.For over-the-counter products, carefully read the package instructions to make sure the product is right for you. Check the ingredients on the label even if you have used the product before. The manufacturer may have changed the ingredients. Also, products with similar brand names may contain different ingredients meant for different purposes. Taking the wrong product could harm you.
HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking esomeprazole and each time you get a refill. If you have any questions, ask your doctor or pharmacist.If you are taking the over-the-counter product to self-treat, read and follow all directions on the product package before taking this medication. If you have any questions, consult your pharmacist. If your doctor has prescribed this medication, take it as directed, usually once daily. Do not crush or chew this medication. Swallow the tablets whole.The dosage and length of treatment are based on your medical condition and response to treatment. Do not increase your dose or take this drug more often than directed. If you have any questions, ask your doctor or pharmacist.If needed, antacids may be taken along with this medication. If you are also taking sucralfate, take esomeprazole at least 30 minutes before sucralfate.Use this medication regularly to get the most benefit from it. To help you remember, take it at the same time each day. Continue to take this medication for the prescribed length of treatment even if you are feeling better. If you are self-treating with the over-the-counter product, do not take it for more than 14 days unless directed by your doctor.Tell your doctor if your condition lasts or gets worse. If you are self-treating, tell your doctor if your heartburn lasts after 14 days or if you need to use this medication more than once every 4 months. The risk of side effects goes up over time. Ask your doctor how long you should take this medication. If you think you may have a serious medical problem, get medical help right away.
SIDE EFFECTS: See also Precautions section.Headache or abdominal pain may occur. If any of these effects last or get worse, tell your doctor or pharmacist promptly.If your doctor has directed you to use this medication, remember that your doctor has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor right away if you have any serious side effects, including: symptoms of a low magnesium blood level (such as muscle spasms, irregular heartbeat, seizures), signs of lupus (such as rash on nose and cheeks, new or worsening joint pain).This medication may rarely cause a severe intestinal condition due to a bacteria called C. difficile. This condition may occur during treatment or weeks to months after treatment has stopped. Tell your doctor right away if you develop: diarrhea that doesn't stop, abdominal or stomach pain/cramping, blood/mucus in your stool.If you have these symptoms, do not use anti-diarrhea or opioid products because they may make symptoms worse.Rarely, proton pump inhibitors (such as esomeprazole) have caused vitamin B-12 deficiency. The risk is increased if they are taken every day for a long time (3 years or longer). Tell your doctor right away if you develop symptoms of vitamin B-12 deficiency (such as unusual weakness, sore tongue, or numbness/tingling of the hands/feet).A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: fever, swollen lymph nodes, rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing, signs of kidney problems (such as change in the amount of urine).This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.
PRECAUTIONS: Before taking esomeprazole, tell your doctor or pharmacist if you are allergic to it; or to other PPIs (such as lansoprazole, omeprazole); or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, lupus.Some symptoms may actually be signs of a more serious condition. Get medical help right away if you have: heartburn with lightheadedness/sweating/dizziness, chest/jaw/arm/shoulder pain (especially with shortness of breath, unusual sweating), unexplained weight loss.In addition, before you self-treat with this medication, get medical help right away if you have any of these signs of a serious condition: trouble/pain swallowing food, bloody vomit, vomit that looks like coffee grounds, bloody/black stools, heartburn for over 3 months, frequent chest pain, frequent wheezing (especially with heartburn), nausea/vomiting, stomach pain.Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).Proton pump inhibitors (such as esomeprazole) may increase your risk for bone fractures, especially with longer use, higher doses, and in older adults. Talk with your doctor or pharmacist about ways to prevent bone loss/fracture, such as by taking calcium (such as calcium citrate) and vitamin D supplements.Older adults may be more sensitive to the side effects of this drug, especially bone loss and fractures (see above), and C. difficile infection (see Side Effects section).Children may be more sensitive to the side effects of this drug, especially fever, cough, and infections of the nose/throat/airways.During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is unknown if this medication passes into breast milk. However, similar drugs pass into breast milk. The effects on a nursing infant are unknown. Consult your doctor before breast-feeding.
DRUG INTERACTIONS: See also How to Use section.Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.Some products that may interact with this drug include: cilostazol, clopidogrel, methotrexate (especially high-dose treatment), rifampin, St John's wort.Some products need stomach acid so that the body can absorb them properly. Esomeprazole decreases stomach acid, so it may change how well these products work. Some affected products include atazanavir, erlotinib, nelfinavir, rilpivirine, certain azole antifungals (itraconazole, ketoconazole, posaconazole), levoketoconazole, pazopanib, among others.Esomeprazole is very similar to omeprazole. Do not use any medications containing omeprazole while using esomeprazole.This medication may interfere with certain laboratory tests, possibly causing false test results. Make sure laboratory personnel and all your doctors know you use this drug.
OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center. Symptoms of overdose may include: confusion, extreme sweating, blurred vision, or unusually fast heartbeat.
NOTES: If your doctor has prescribed this medication for you, do not share it with others.If your doctor instructs you to use this medication regularly for a long time, laboratory and medical tests (such as a magnesium blood test, vitamin B-12 levels) may be performed periodically to monitor your progress or check for side effects. Keep all regular medical and laboratory appointments.
MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose. Take your next dose at the regular time. Do not double the dose to catch up.
STORAGE: Store at room temperature away from moisture. Do not store in the bathroom. Keep all medications away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company.
Information last revised April 2022. Copyright(c) 2022 First Databank, Inc.
IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.
Formulary
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Adding plans allows you to:
- View the formulary and any restrictions for each plan.
- Manage and view all your plans together – even plans in different states.
- Compare formulary status to other drugs in the same class.
- Access your plan list on any device – mobile or desktop.
