See Available Brands of Esomeprazole in India

P - Caution when used during pregnancy
L - Caution when used during lactation
FI - Food *
LI - Lab *

Esomeprazole is a proton pump inhibitor (brand names Sompraz, Zoleri, Nexium®, Lucen, Esopral; Axagon in Italy, Nexiam in Belgium) developed and marketed by AstraZeneca which is used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and Zollinger-Ellison syndrome. Esomeprazole is the S-enantiomer of omeprazole (marketed as Losec/Prilosec), and AstraZeneca claims improved efficacy of this single enantiomer product over the racemic mixture of omeprazole.

Pharmacodynamics

Pharmacokinetics

Esomeprazole is a PPI that suppresses gastric acid secretion by specific inhibition of the H+/K+ ATPase in the gastric parietal cell.
Absorption
Rapid (oral). Peak plasma levels after 1-2 hours; food delays and decreases absorption.

Distribution
Protein-binding: 97%

Metabolism
Extensively hepatic; converted to hydroxy and desmethyl metabolites.

Excretion
Urine (as metabolites); 1.3 hours (elimination half-life).

Esomeprazole Indications / Esomeprazole Uses

Information Not Available

Esomeprazole Adverse Reactions / Esomeprazole Side Effects

Headache, diarrhoea, abdominal pain, nausea, flatulence, dry mouth, constipation, hyponatraemia, photosensitivity, angioedema, anaphylaxis.

Precautions

Hypersensitivity

May occur; angioedema and anaphylactic reaction/shock have been reported.

Atrophic gastritis
Has been reported in patients receiving long-term treatment with omeprazole, of which esomeprazole is an enantiomer.

Overdosage
Symptoms
Blurred vision, confusion, diaphoresis, drowsiness, dry mouth, flushing, headache, nausea, tachycardia.

Special Precautions

Paediatric; pregnancy, lactation. Malignancy and hepatic impairment. Increased risk of developing certain infections such as community-acquired pneumonia.

Other Drug Interactions

May interfere with the elimination of drugs metabolised by CYP2C19. Changes in gastric pH can affect the bioavailability of ketoconazole and Fe salts. Clarithromycin and amoxicillin may increase plasma level. May cause changes to prothrombin time when used with warfarin.

Other Interactions

Food Interaction
Absorption delayed with food.

Dosage

Oral
Erosive oesophagitis
Adult: 40 mg once daily for 4 wk, extended for another 4 wk if necessary. Maintenance: 20 mg once daily.
Child: <20 kg: 10 mg once daily for 8 wk; ≥20 kg: 10-20 mg once daily for 8 wk.
Hepatic impairment: Severe impairment (Child-Pugh class C): Not more than 20 mg daily.

Oral
Peptic ulcer
Adult: 20 mg bid for 7 days or 40 mg once daily for 10 days given as a triple therapy with amoxicillin and clarithromycin.
Hepatic impairment: Severe impairment (Child-Pugh class C): Not more than 20 mg daily.

Oral
NSAID-associated ulceration
Adult: 20 mg once daily for 4-8 wk.
Hepatic impairment: Severe impairment (Child-Pugh class C): Not more than 20 mg daily.

Oral
Zollinger-Ellison syndrome
Adult: Initially, 40 mg twice daily. Usual range: 80-160 mg daily. Doses >80 mg should be given in 2 divided doses.
Hepatic impairment: Severe impairment (Child-Pugh class C): Not more than 20 mg daily.

Oral
Gastro-oesophageal reflux disease
Adult: For patients without erosive oesophagitis: 20 mg once daily for 4 wk. Additional 4 wk may be considered in patients whose symptoms have not fully resolved after the 1st course.
Child: 10 mg once daily for up to 8 wk.
Hepatic impairment: Severe impairment (Child-Pugh class C): Not more than 20 mg daily.

Intravenous
Gastro-oesophageal reflux disease
Adult: For short term treatment only. 20 or 40 mg once daily for ≤10 days. Convert to oral therapy as soon as possible. May be administered by inj over at least 3 minutes, intermittent infusion (10-30 minutes) or continuous infusion (over up to 72 hr).
Hepatic impairment: Severe impairment (Child-Pugh class C): Not more than 20 mg daily.

Reconstitution
Each single-use vial contains 20 or 40 mg of esomeprazole. For IV inj: Reconstitute each vial with 5 ml of normal saline. For IV infusion: Reconstitute each vial with 5 ml of normal saline, lactated Ringer's inj or dextrose 5% inj, then further dilute the resultant solution to a final volume of 50 ml.

Food(before/after)

Delayed-release cap: Should be taken on an empty stomach. (Take on an empty stomach 1 hr before meals.)
Tab: May be taken with or without food.

List of Contraindications

Esomeprazole and Pregnancy

Caution when used during pregnancy.

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Esomeprazole and Lactation

Caution when used during lactation

Esomeprazole and Children

Information Not Available

Esomeprazole and Geriatic

Information Not Available

Esomeprazole and Other Contraindications

Hypersensitivity

Storage

Intravenous
Pwd for inj:
Store at 25°C (77°F). Protect from light. Reconstituted solution for inj should be stored at room temperature up to 30°C and administered within 12 hr after preparation. Reconstituted solution for infusion should be stored at room temperature up to 30°C and administered within 12 hr (if normal saline or lactated Ringer's inj is used as the diluent) or 6 hr (if dextrose 5% inj is used as the diluent).

Oral
Store at 25°C.

Lab interference

Increased creatinine, uric acid, bilirubin, alkaline phosphatase, ALT, AST. Altered thyroid function tests.