Esomeprazole
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Esomeprazole
Nexium, Nexium 24HR (OTC)
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Summary
Common uses
GERD0, Erosive esophagitis (healing and maintenance)0, H. pylori eradication (combination)0, Zollinger-Ellison syndrome0, NSAID-associated ulcer prophylaxis0
Pharmacy
Starting dose
20-40 mg PO once daily, 30-60 minutes before breakfast
Preparations
20, 40 mg delayed-release capsules; 2.5, 5, 10, 20, 40 mg oral suspension packets; 20, 40 mg IV
US FDA Max
40 mg/d typical; up to 240 mg/d for Zollinger-Ellison
Pharmacology
Routes
Oral, IV
Onset
Acid suppression within hours; full effect after 3-5 days of dosing
Duration
24-72 hours per dose (irreversible enzyme binding)
Half-life
~1.5 hours (plasma); pharmacodynamic effect 24+ hours via target turnover[2]
Bioavailability
~64-90% (oral; increases at higher doses and with multi-day dosing)[2]
Pregnancy
Widely used in obstetric reflux; reassuring data.[citation needed]
Legal status
OTC (20 mg, 14-day course) and Rx-only (higher and longer durations) in US
Purported mechanism
Esomeprazole is the S-enantiomer of omeprazole; chiral separation reduces inter-individual variability driven by CYP2C19-mediated R-enantiomer clearance, yielding more consistent acid suppression than racemic omeprazole, particularly in CYP2C19 extensive metabolizers.0 Like omeprazole, it is an acid-activated prodrug that covalently and irreversibly binds the H+/K+ ATPase. CYP2C19 PGx remains clinically relevant for both[1].
References
- ↑ CPIC Guideline for CYP2C19 and Proton Pump Inhibitors, 2020. https://cpicpgx.org/guidelines/cpic-guideline-for-proton-pump-inhibitors-and-cyp2c19/
- ↑ 2.0 2.1 FDA Prescribing Information, Nexium (esomeprazole magnesium), AstraZeneca, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2014/021153s050,021957s017,022101s014,021689s029,022101s009lbl.pdf