ESOMEPRAZOLE SODIUM
Clinical safety rating: safe
Can reduce absorption of drugs requiring gastric pH for absorption (eg ketoconazole) May increase risk of Clostridium difficile-associated diarrhea and bone fractures with long-term use.
Proton pump inhibitor that irreversibly inhibits the H+/K+-ATPase enzyme system (proton pump) in gastric parietal cells, suppressing gastric acid secretion.
| Metabolism | Primarily hepatic via CYP2C19 and CYP3A4 isoenzymes; CYP2C19 is the major pathway, converting esomeprazole to hydroxyl and desmethyl metabolites (inactive). |
| Excretion | Primarily hepatic metabolism (~80%) via CYP2C19 and CYP3A4; renal excretion of inactive metabolites accounts for ~80% of an oral dose, with ~20% excreted in feces via bile. |
| Half-life | Terminal elimination half-life is approximately 1–1.5 hours in healthy individuals; clinical context: longer half-life (~2–3 hours) in slow CYP2C19 metabolizers, but acid suppression lasts longer due to irreversible binding to H+/K+-ATPase. |
| Protein binding | Approximately 97% bound to albumin; minimal binding to alpha1-acid glycoprotein. |
| Volume of Distribution | Steady-state Vd is 0.22–0.26 L/kg; low Vd indicates limited extravascular distribution, consistent with high protein binding and compartmentalization into gastric parietal cells. |
| Bioavailability | Oral delayed-release: ~64% (range 50–90%) on repeated dosing; intravenous: 100%. |
| Onset of Action | Intravenous: 30–60 minutes for gastric acid suppression; oral (delayed-release): 1–4 hours for measurable effect, with maximal acid suppression within 3–5 days of repeated dosing. |
| Duration of Action | Acid suppression persists for up to 24–72 hours after single dose due to irreversible enzyme inhibition; full recovery of gastric acid secretion occurs over 3–5 days after discontinuation. |
20-40 mg IV once daily for up to 10 days; oral: 20-40 mg once daily for 4-8 weeks for erosive esophagitis, 20 mg once daily for gastroesophageal reflux disease.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (CrCl >30 mL/min). For severe renal impairment (CrCl <30 mL/min), maximum dose is 20 mg daily. |
| Liver impairment | Child-Pugh A: No adjustment. Child-Pugh B: Maximum dose 20 mg daily. Child-Pugh C: Not recommended; limited data. |
| Pediatric use | For GERD: 1-11 months: 0.5-1 mg/kg once daily; 1-17 years: 10-20 mg once daily (weight <20 kg: 10 mg; ≥20 kg: 20 mg). For erosive esophagitis: 1-17 years: 10-20 mg once daily for 8 weeks. |
| Geriatric use | No specific dose adjustment required; however, consider lower starting doses (20 mg daily) due to potential age-related decline in renal function and increased risk of adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Can reduce absorption of drugs requiring gastric pH for absorption (eg ketoconazole) May increase risk of Clostridium difficile-associated diarrhea and bone fractures with long-term use.
| FDA category | Animal |
| Breastfeeding | Esomeprazole is excreted into human milk in low concentrations; the estimated infant dose is <1% of maternal weight-adjusted dose. M/P ratio not reported. Short-term use is considered compatible with breastfeeding. Monitor infant for irritability, feeding intolerance, or excess sleepiness. |
| Teratogenic Risk |
■ FDA Black Box Warning
None.
| Common Effects | erosive esophagitis |
| Serious Effects |
["Hypersensitivity to esomeprazole or substituted benzimidazoles","Concomitant use with rilpivirine","Concomitant use with methotrexate (high dose)"]
| Precautions | ["Gastric malignancy risk (symptomatic response may mask underlying neoplasia)","Clostridium difficile-associated diarrhea (increased risk with prolonged use)","Osteoporosis-related fractures (hip, wrist, spine) with long-term high-dose use","Hypomagnesemia (symptomatic, especially with prolonged use; monitor magnesium levels)","CYP2C19 poor metabolizers (increased drug exposure)","Acute interstitial nephritis","Vitamin B12 deficiency (chronic use may impair absorption)","Interaction with clopidogrel (reduced antiplatelet effect; coadministration not recommended)"] |
Loading safety data…
| Esomeprazole is a proton pump inhibitor with low teratogenic risk. First trimester: No increased risk of major congenital malformations based on large cohort studies. Second and third trimesters: No documented fetal toxicity. However, use only if clearly needed due to inadequate data. |
| Fetal Monitoring | Monitor maternal symptom relief and adverse effects (headache, diarrhea, abdominal pain). No specific fetal monitoring required. For prolonged use, assess maternal bone mineral density and magnesium levels periodically. In third trimester, watch for early neonatal respiratory distress if used near term? (No specific data). |
| Fertility Effects | No evidence of impaired fertility in animal studies. In humans, no known adverse effects on male or female fertility. Proton pump inhibitors are not associated with infertility. |