Esomeprazole

ATC code

A02BC05

Therapeutic class

Proton pump inhibitor · Drugs for peptic ulcer and gastro-oesophageal reflux disease

Forms

gastro-resistant tablet

Brand names

Nexium Control (EU) · AXIAGO (ES) · ESOMEPRAZOLE CRISTERS PHARMA (FR) · Acid Reducer (US)

Overall confidence

high

Regulatory sources consulted

openfda-label-5f0bc616-6126-4f48-b56c-e8874aed6e90
aemps-ft-63940
ansm-rcp-65058282
ema-epar-EMEA/H/C/002618
PubMed PMID:36142643 ↗
PubMed PMID:35787720 ↗
PubMed PMID:38345252 ↗
CredibleMeds.org
OpenFDA · A02BC05
RxNorm rxcui 283742 ↗

Approved indications

Short-term treatment of reflux symptoms (e.g. heartburn and acid regurgitation) in adults.
Gastroesophageal reflux disease (GERD).
Eradication of Helicobacter pylori in combination with an appropriate antibacterial therapeutic regimen.
Treatment of Zollinger-Ellison syndrome.

Contraindications

Absolute

Hypersensitivity to esomeprazole, substituted benzimidazoles or to any of the excipients.
Esomeprazole should not be used concomitantly with nelfinavir.

Clinical warnings

Long-term use (>1 year) may modestly increase the risk of hip, wrist and spine fracture, predominantly in the elderly or in presence of other risk factors. — EMA SPC
Major warning · Severe hypomagnesaemia has been reported in patients treated with PPIs for at least three months. It can manifest with fatigue, tetany, delirium, convulsions, dizziness and ventricular arrhythmia. — EMA SPC
Treatment with PPIs may lead to a slightly increased risk of gastrointestinal infections such as Salmonella and Campylobacter. — EMA SPC
PPIs are associated with very infrequent cases of subacute cutaneous lupus erythematosus (SCLE). — EMA SPC

Drug interactions

ModerateClopidogrelB01AC04
Mechanism: Esomeprazole is a potent inhibitor of CYP2C19, the enzyme that activates the prodrug clopidogrel. Co-administration reduces exposure to the active metabolite of clopidogrel and diminishes its antiplatelet effect.
Recommendation: Avoid concomitant use. Consider an alternative PPI with less CYP2C19 inhibition (e.g., pantoprazole) or an alternative antiplatelet agent if a PPI is required.
PMID:35787720EMA SPC
ModerateMethotrexateL01BA01
Mechanism: Increased methotrexate levels have been reported. The exact mechanism is unclear but may involve inhibition of renal tubular secretion.
Recommendation: In patients receiving high-dose methotrexate, a temporary withdrawal of esomeprazole may be considered. Monitor for methotrexate levels and toxicity.
ANSM RCP
ModerateTacrolimusL04AD02
Mechanism: Concomitant administration may increase serum tacrolimus levels, likely through inhibition of its metabolism via CYP3A4 and/or CYP2C19.
Recommendation: Reinforced monitoring of tacrolimus concentrations and renal function (creatinine clearance) should be performed; adjust tacrolimus dosage if necessary.
ANSM RCP

Adverse events

Common (≥1%)

headache · abdominal pain · diarrhoea · nausea · flatulence

Rare but serious

agranulocytosis · pancytopenia · anaphylactic reaction/shock · severe hypomagnesemia · interstitial nephritis · Stevens-Johnson syndrome · subacute cutaneous lupus erythematosus

Pregnancy and lactation

Pregnancy: Clinical data on exposed pregnancies are insufficient. Animal studies do not indicate harmful effects. Use with caution. Lactation: It is unknown whether it is excreted in human milk. Should not be used during breast-feeding.

Recent literature (PubMed)

An update on drug-drug interactions associated with proton pump inhibitors.
Ben Ghezala I, et al. · Expert Opin Drug Metab Toxicol · 2022 · Relevance 5/5
Revisión actualizada de las interacciones farmacológicas de los IBP. Destaca que esomeprazol es un potente inhibidor de CYP2C19, a diferencia de pantoprazol o rabeprazol, lo que es clave para interacciones clínicamente significativas (p. ej., con clopidogrel).
Comparative Efficacy of P-CAB vs Proton Pump Inhibitors for Grade C/D Esophagitis: A Systematic Review and Network Meta-analysis.
Zhuang Q, et al. · Am J Gastroenterol · 2024 · Relevance 5/5
Metaanálisis en red que compara los bloqueadores de ácido competitivos con potasio (P-CAB) con los IBP para la esofagitis grave. Vonoprazan (un P-CAB) demostró una eficacia superior a los IBP, incluido el esomeprazol, en la curación inicial y de mantenimiento de la esofagitis C/D, con un perfil de seguridad similar a corto y largo plazo.
Proton Pump Inhibitors and Bone Health: An Update Narrative Review.
Lespessailles E, et al. · Int J Mol Sci · 2022 · Relevance 4/5
Revisión narrativa sobre la asociación entre el uso de IBP y la salud ósea. Resume la evidencia sustancial de estudios observacionales que vinculan el uso a largo plazo de IBP con un mayor riesgo de fracturas osteoporóticas, aunque los mecanismos subyacentes y el efecto sobre la DMO no están completamente elucidados.