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Drug Reference

esomeprazole

Proton pump inhibitor· Brands: NexiumIVPO

Mechanism of action
Esomeprazole is a proton pump inhibitor that irreversibly blocks the gastric H+/K+-ATPase enzyme in parietal cells, thereby suppressing gastric acid secretion. It is the S-isomer of omeprazole and provides more consistent acid suppression than the racemic mixture.
Pharmacokinetics
Esomeprazole is acid-labile, so it is formulated as enteric-coated granules. After oral administration, absorption is rapid, with peak plasma concentrations occurring within 1 to 2 hours. It undergoes extensive hepatic metabolism via CYP2C19 and CYP3A4, with the S-isomer being less affected by CYP2C19 polymorphisms than omeprazole. The elimination half-life is approximately 1.3 hours, but the antisecretory effect persists longer because of irreversible enzyme inhibition. It is excreted mainly in urine as metabolites.
Indications & dosing

Gastro-oesophageal reflux disease

Short-term treatment; moderate-severe symptoms may require 40 mg.

  • adult · PO: 20–40 mg once daily · Short-term treatment; moderate-severe symptoms may require 40 mg.

Erosive oesophagitis

Healing and symptom relief; course of 4-8 weeks.

  • adult · PO: 20–40 mg once daily · Healing and symptom relief; course of 4-8 weeks.

Helicobacter pylori eradication (combination therapy)

Given with antibiotics for 7-14 days.

  • adult · PO: 20 mg twice daily · Given with antibiotics for 7-14 days.

NSAID-induced ulcer prophylaxis

In patients requiring long-term NSAIDs.

  • adult · PO: 20 mg once daily · In patients requiring long-term NSAIDs.

Zollinger-Ellison syndrome

Dosage individualised; may require higher doses given in divided doses.

  • adult · PO: 40–120 mg once daily · Dosage individualised; may require higher doses given in divided doses.

Erosive oesophagitis in children (12-17 years)

Same dosing as adults; course 4-8 weeks.

  • pediatric · PO: 20–40 mg once daily · Same dosing as adults; course 4-8 weeks.
Contraindications & precautions
  • Hypersensitivity to esomeprazole, other proton pump inhibitors, or any excipient · Includes anaphylaxis, angioedema, bronchospasm, and dermatologic reactions.
  • Concomitant use with atazanavir or nelfinavir · PPIs significantly reduce the absorption of these antiretroviral agents, leading to loss of virologic response.
  • Concomitant use with rilpivirine · Rilpivirine requires an acidic gastric environment for adequate absorption; PPIs reduce its plasma concentrations.
  • Long-term use: monitor for vitamin B12 deficiency, hypomagnesemia, and bone mineral density loss; use lowest effective dose for shortest duration.
  • Concomitant use with clopidogrel: esomeprazole may reduce clopidogrel activation via CYP2C19 inhibition; consider alternative acid-suppressive therapy.
  • Before initiating therapy for gastric symptoms, exclude gastric malignancy: esomeprazole may mask symptoms of gastric cancer.
  • Hepatic impairment: in severe impairment (Child-Pugh C), do not exceed 20 mg daily.
  • Pregnancy and breastfeeding: limited safety data; use only if clearly needed and benefits outweigh potential risks.
  • Rebound acid hypersecretion may occur upon discontinuation; if stopping after long-term therapy, taper gradually.
Adverse effects
  • Headache
  • Abdominal pain
  • Diarrhoea
  • Nausea
  • Dizziness
  • Interstitial nephritisserious
  • Hepatic failureserious
  • Hypomagnesaemiaserious
Interactions
  • clopidogrelmajorAvoid co-prescription when possible. If a proton pump inhibitor is needed, consider using pantoprazole, which has minimal CYP2C19 inhibition, or an alternative antiplatelet agent such as ticagrelor or prasugrel. If the combination is considered necessary, monitor patients closely for signs of cardiovascular events and assess platelet function if available.
Renal & hepatic adjustment
  • Hepatic impairment (mild): No dose adjustment required
  • Hepatic impairment (moderate): No dose adjustment required
  • Hepatic impairment (severe): Maximum daily dose of 20 mg
Monitoring, pregnancy & toxicity
  • Symptom response (heartburn, dyspepsia) · At 4 to 8 weeks after starting treatment
  • Serum magnesium · Before and periodically during long-term therapy, especially if co-prescribed with diuretics
  • Liver function tests · In patients with severe hepatic impairment
  • Serum vitamin B12 · Consider in patients on long-term therapy
  • Pregnancy: Esomeprazole is not known to be harmful in pregnancy; use if clinically indicated. In lactation, it is excreted in breast milk but at low levels, and is generally considered compatible with breastfeeding.
  • Toxicity: Symptoms of overdose: nausea, vomiting, abdominal pain, diarrhoea, headache, dizziness, confusion, dry mouth, blurred vision, sweating, tachycardia, hyperventilation, and rarely seizures. · Supportive care; no specific antidote. Monitor vital signs and electrolytes. Activated charcoal may be considered if ingestion is recent and patient is stable.
Clinical notes
Esomeprazole is indicated for gastro-oesophageal reflux disease, peptic ulcer disease, and Helicobacter pylori eradication in combination with antibiotics. It is also used for the prevention of NSAID-associated ulcers. The intravenous form is used when oral therapy is not possible. It is generally well tolerated, with headache, gastrointestinal upset, and hypomagnesaemia on prolonged use. Long-term use may be associated with an increased risk of fractures and Clostridioides difficile infection. Dose adjustment is not required for renal or mild hepatic impairment, but caution is advised in severe hepatic impairment.

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BNF; local formulary