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. |
| Molecular Weight | 345.42 |
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 | Esomeprazole is generally considered safe during the first trimester; animal studies show no evidence of teratogenicity, and human data do not indicate an increased risk of major birth defects. |
| 2nd trimester | No known risks in the second trimester; use if clearly needed. |
| 3rd trimester | No known risks in the third trimester; use if clearly needed. |
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 |
| Placental transfer | Esomeprazole crosses the placenta; based on its molecular weight and pharmacokinetics, limited placental transfer occurs, but specific quantitative data are lacking. |
■ FDA Black Box Warning
None.
| Common Effects | erosive esophagitis |
| Serious Effects |
History of hypersensitivity to esomeprazole or any component of the formulationUse with rilpivirine-containing productsUse with nelfinavir
| 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) |
| Food/Dietary |
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| Breastfeeding |
| Esomeprazole is excreted into human breast milk in low amounts. The estimated infant dose is less than 1% of the maternal weight-adjusted dose. No adverse effects have been reported in breastfed infants. Caution is advised, but it is generally considered compatible with breastfeeding. |
| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | 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. |
| Esomeprazole absorption is reduced by food; administer at least 1 hour before a meal. High-fat meals may delay absorption. Avoid excessive alcohol and spicy foods that may exacerbate symptoms. No specific food restrictions, but patients should follow a diet that minimizes acid reflux triggers (e.g., citrus, tomatoes, caffeine, chocolate, mint, onions, and fatty or fried foods). |
| Clinical Pearls | Administer IV esomeprazole as a slow injection (over 3 minutes) or infusion (10-30 minutes). For stress ulcer prophylaxis in critically ill patients, consider continuous infusion after a bolus. Esomeprazole is the S-isomer of omeprazole; it undergoes less first-pass metabolism, yielding higher and more predictable bioavailability. Use with caution in patients with hepatic impairment (reduce dose in severe disease). Monitor for hypomagnesemia with prolonged use (>1 year). Coadministration with clopidogrel may reduce antiplatelet effect; avoid combination if alternative PPI available. |
| Patient Advice | Take esomeprazole exactly as prescribed; do not crush or chew delayed-release capsules. · Swallow the capsule whole with a glass of water; if you have trouble swallowing, you can open the capsule and mix the contents with applesauce. · Take the medication at least 1 hour before a meal for best results. · Do not double a missed dose; skip it and resume your regular schedule. · Notify your healthcare provider if you experience severe diarrhea, joint pain, or rash. · Long-term use may increase risk of bone fractures, vitamin B12 deficiency, and kidney inflammation. · Avoid taking with St. John's wort, rifampin, or methotrexate without doctor approval. |