Trade Names:Nexium- Capsules, delayed-release 20 mg- Capsules, delayed-release 40 mg
Trade Names:Nexium- Powder for suspension, delayed-release 10 mg- Powder for suspension, delayed-release 20 mg- Powder for suspension, delayed-release 40 mgEsomeprazole Sodium
Trade Names:Nexium I.V.- Injection 20 mg- Injection 40 mg
Suppresses gastric acid secretion by blocking proton pump within gastric parietal cells.
T max is 1.5 h. Bioavailability is approximately 90% (repeated once-daily dosing) and 64% (single dose). Food decreases AUC by 43% to 53%. C max following IV administration of 20 and 40 mg for 5 days is 3.86 and 7.51 mcmol/L, respectively.
Esomeprazole is 97% protein bound. Vd is approximately 16 L (at steady state).
Metabolized in the liver by CYP2C19 and CYP3A4 to inactive metabolites.
The half-life is approximately 1 to 1.5 h. Less than 1% of parent drug excreted in urine; approximately 80% excreted as inactive metabolites in the urine, and the remainder is found in feces.
Less than 1% of the dose is excreted unchanged in the urine. Dosage adjustment is not necessary.Hepatic Function Impairment
AUC was 2 to 3 times higher in patients with severe hepatic function impairment.Elderly
AUC and C max were increased by 25% and 18%, respectively. Dosage adjustment is not necessary.Gender
AUC and C max were higher (13%) in women than men. Dosage adjustment is not necessary.
Treatment of heartburn and other symptoms of gastroesophageal reflux disease (GERD); short-term treatment in healing and symptomatic resolution of erosive esophagitis; maintenance of symptom resolution and healing of erosive esophagitis; in combination with amoxicillin and clarithromycin for treatment of Helicobacter pylori infection and duodenal ulcer disease to eradicate H. pylori ; reduction in occurrence of gastric ulcers associated with continuous NSAID therapy in patients at risk of developing gastric ulcers; long-term treatment of pathological hypersecretory conditions, including Zollinger-Ellison syndrome.IV
As an alternative to oral therapy when oral therapy with esomeprazole delayed-release capsules is not possible or appropriate for the short-term treatment (up to 10 days) of GERD in patients with history of erosive esophagitis.
Non-GERD dyspepsia; Barrett esophagus; stress ulcer prophylaxis (oral); stress ulcer prophylaxis (IV).
Hypersensitivity to any component of the formulation or to substituted benzimidazoles.
PO 20 or 40 mg once daily for 4 to 8 wk. For patients who do not heal after 4 to 8 wk, consider an additional 4 to 8 wk of treatment.Children 1 to 11 yr of age PO Weight of less than 20 kg
Administer 10 mg once daily for 8 wk.Weight of 20 kg or more
Administer 10 or 20 mg once daily for 8 wk.H. Pylori Eradication to Reduce Risk of Duodenal Ulcer RecurrenceAdults
PO 40 mg once daily for 10 days in combination with amoxicillin 1,000 mg twice daily and clarithromycin 500 mg twice daily for 10 days.GERD With History of Erosive EsophagitisAdults
IV 20 or 40 mg once daily.Maintenance of Healing of Erosive EsophagitisAdults
PO 20 mg once daily.Pathological Hypersecretory Conditions Including Zollinger-Ellison SyndromeAdults
PO 40 mg twice daily.Risk Reduction of NSAID-Associated Gastric UlcerAdults
PO 20 or 40 mg once daily for up to 6 mo.Short-Term Treatment of GERDChildren 12 to 17 yr of age
PO 20 or 40 mg once daily for up to 8 wk.Children 1 to 11 yr of age
PO 10 mg once daily for up to 8 wk.Symptomatic GERDAdults
PO 20 mg once daily for 4 wk. If symptoms do not resolve after 4 wk, an additional 4 wk of treatment may be considered.Hepatic Function Impairment
For severe impairment (Child-Pugh class C), do not exceed a dose of 20 mg.
Store capsules and suspension at 59° to 86°F. Keep container tightly closed.IV
Store vials for injection at 59° to 86°F. Administer reconstituted solution within 12 h after reconstitution. Administer IV infusion within 12 h after mixing with sodium chloride 0.9% injection or Ringer's lactate injection or 6 h after mixing with dextrose 5% injection. Protect from light. Store in carton until time of use.
Plasma concentrations may be reduced by esomeprazole, decreasing the efficacy. Avoid coadministration.Clarithromycin, voriconazole
Esomeprazole plasma concentrations may be elevated, increasing the pharmacologic effects and adverse reactions.Clopidogrel
The antiplatelet activity of clopidogrel may be decreased. Avoid coadministration unless there is a specific indication for a proton pump inhibitor. H 2 - receptor antagonists (eg, ranitidine) may be a safer alternative.Diazepam
Plasma concentrations may be increased by esomeprazole; however, the increase is not likely to be clinically important.Drugs dependent on gastric pH for bioavailability (eg, digoxin, iron salts, ketoconazole)
Absorption of these drugs may be affected (eg, digoxin concentrations may be increased, itraconazole and ketoconazole concentrations may be decreased).Tolterodine
Plasma concentrations may be elevated by esomeprazole, increasing the pharmacologic effects and adverse reactions. Closely monitor the patient and adjust the tolterodine dose as needed.Warfarin
Risk of bleeding may be increased.
None well documented.
Headache (11%); dizziness (3%); somnolence (2%); aggression, agitation, depression, hallucination (postmarketing).
Pruritus (1%); alopecia, erythema multiforme, hyperhidrosis, photosensitivity, Stevens-Johnson syndrome, toxic epidermal necrolysis (postmarketing).
Blurred vision (postmarketing).
Flatulence (10%); abdominal pain, dyspepsia, nausea (6%); diarrhea, dry mouth (4%); constipation (3%); GI candidiasis, pancreatitis, stomatitis, taste disturbance (postmarketing).
Gynecomastia, interstitial nephritis (postmarketing).
Hepatic encephalopathy, hepatic failure, hepatitis with or without jaundice (postmarketing).
Agranulocytosis, pancytopenia (postmarketing).
Increased alkaline phosphate, ALT, AST, hemoglobin, creatinine, platelets, potassium, serum gastrin, sodium, thyroxine, total bilirubin, TSH, uric acid, and WBC. Decreased hemoglobin, platelets, potassium, sodium, thyroxine, and WBC.
Application-site reactions including mild local erythema and pruritus with IV administration (2%).
Muscular weakness, myalgia (postmarketing).
Sinusitis (2%); respiratory tract infection (1%); bronchospasm (postmarketing).
Anaphylactic reaction/shock (postmarketing).
Category B .
Safety and efficacy not established for uses other than short-term treatment of GERD. In the short-term treatment of GERD, safety and efficacy not established in children younger than 1 yr of age.IV
Safety and efficacy not established.
No differences in safety and efficacy have been observed between elderly and younger patients.
May occur; angioedema and anaphylactic reaction/shock have been reported.
Has been reported in patients receiving long-term treatment with omeprazole, of which esomeprazole is an enantiomer.
Blurred vision, confusion, diaphoresis, drowsiness, dry mouth, flushing, headache, nausea, tachycardia.
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