ESOMEPRAZOLE STRONTIUM
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 inhibits the H+/K+ ATPase in gastric parietal cells, suppressing gastric acid secretion.
| Metabolism | Primarily hepatic via CYP2C19 and CYP3A4; metabolites are inactive. |
| Excretion | Primarily hepatic metabolism via CYP2C19 and CYP3A4. Approximately 80% of metabolites are excreted in urine and 20% in feces via bile. Less than 1% excreted unchanged. |
| Half-life | Terminal elimination half-life: 1.0–1.5 hours in healthy subjects; prolonged in poor CYP2C19 metabolizers (up to 3.5 hours). |
| Protein binding | 97% bound to human plasma proteins (primarily albumin). |
| Volume of Distribution | Apparent Vd: 0.2–0.3 L/kg; indicates low tissue distribution. |
| Bioavailability | Oral: 50–70% after repeated dosing; <1% after first dose due to first-pass metabolism. |
| Onset of Action | Oral: 1 hour for measurable acid suppression; maximal effect achieved after 2–4 days of once-daily dosing. |
| Duration of Action | Acid suppression persists for 24 hours with once-daily dosing; maximal effect after 3–4 days. |
| Molecular Weight | 345.4 |
40 mg orally once daily; for healing of erosive esophagitis, 40 mg orally once daily for 4-8 weeks; for maintenance of healing of erosive esophagitis, 20 mg orally once daily; for GERD, 20 mg orally once daily; for Helicobacter pylori eradication, 40 mg orally twice daily for 10 days in combination with antibiotics.
| Dosage form | CAPSULE, DELAYED RELEASE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment; data insufficient for severe renal impairment (CrCl <30 mL/min), use with caution. |
| Liver impairment | Child-Pugh Class A (mild): no adjustment; Child-Pugh Class B (moderate): maximum dose 20 mg per day; Child-Pugh Class C (severe): not recommended. |
| Pediatric use | For GERD in children 1-11 years: weight <20 kg, 10 mg orally once daily; weight ≥20 kg, 20 mg orally once daily. For erosive esophagitis in children 12-17 years: 20-40 mg orally once daily for 4-8 weeks. |
| Geriatric use | No specific dose adjustment; use lowest effective dose due to potential for increased exposure and decreased renal function; monitor for adverse effects. |
| 1st trimester | Limited human data; animal studies show no risk. Avoid unless clearly needed. |
| 2nd trimester | Limited human data; animal studies show no risk. Avoid unless clearly needed. |
| 3rd trimester | Limited human data; animal studies show no risk. Avoid unless 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; extent unknown. |
| Breastfeeding | Esomeprazole is excreted in human milk in low amounts; likely compatible with breastfeeding but caution advised. |
■ FDA Black Box Warning
None
| Common Effects | erosive esophagitis |
| Serious Effects |
Hypersensitivity to esomeprazole or substituted benzimidazolesConcomitant use with rilpivirine
| Precautions | Increased risk of Clostridium difficile-associated diarrhea, Bone fracture risk with long-term high-dose use, Hypomagnesemia with prolonged use, Atrophic gastritis with long-term use, Possible interference with diagnostic tests for gastric neuroendocrine tumors, Avoid concomitant use with gastric pH-dependent drugs (e.g., rilpivirine, atazanavir) |
| Food/Dietary | Take on an empty stomach at least 30-60 minutes before a meal. Avoid high-fat meals which may delay absorption. No specific food restrictions, but concurrent use with St. John's wort or high doses of vitamin C may alter drug levels. |
Loading safety data…
| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | Esomeprazole strontium is classified as Pregnancy Category C. In the first trimester, there is insufficient data to determine risk; however, proton pump inhibitors (PPIs) have not been consistently associated with major congenital malformations. In the second and third trimesters, animal studies have shown no teratogenic effects, but human data are limited. Use only if clearly needed. |
| Fetal Monitoring | Monitor maternal renal and hepatic function. Assess for potential vitamin B12 deficiency with long-term use. Fetal monitoring as per standard obstetric care. |
| Fertility Effects | No specific human studies on fertility. Animal studies indicate no impairment of fertility at clinically relevant doses. No known adverse effects on spermatogenesis or oogenesis. |
| Clinical Pearls | Esomeprazole strontium is a delayed-release formulation; capsules should be swallowed whole and not crushed or chewed. Onset of acid suppression is similar to other PPIs, but strontium may be less bioavailable than esomeprazole magnesium. Monitor for hypomagnesemia with prolonged use. Avoid concurrent use with clopidogrel due to potential reduced efficacy. Strontium can cause false elevations in calcium levels on some lab assays. |
| Patient Advice | Take esomeprazole strontium exactly as prescribed, usually once daily 30-60 minutes before a meal. · Swallow the capsule whole; do not crush, chew, or open it. · If you have trouble swallowing, you may open the capsule and sprinkle the contents on a tablespoon of applesauce; swallow immediately without chewing. · Do not take this medication with other acid reducers without consulting your doctor. · Report persistent diarrhea, muscle cramps, or irregular heartbeat (signs of low magnesium). · Long-term use may increase risk of bone fractures, vitamin B12 deficiency, and kidney problems. |