ZEGERID OTC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ZEGERID OTC (ZEGERID OTC).
Omeprazole is a proton pump inhibitor (PPI) that suppresses gastric acid secretion by irreversibly binding to the H+/K+-ATPase enzyme (the proton pump) in the gastric parietal cells.
| Metabolism | Primarily metabolized by CYP2C19 and CYP3A4 in the liver. |
| Excretion | Renal (80% as metabolites) and fecal (20%) |
| Half-life | Terminal half-life approximately 1.5-2 hours (0.5-1 hour in children); due to short half-life, acid suppression duration is prolonged via irreversible proton pump inhibition |
| Protein binding | 97% bound to plasma proteins (primarily albumin and alpha1-acid glycoprotein) |
| Volume of Distribution | Approximately 0.15-0.3 L/kg; low Vd indicates limited extravascular distribution |
| Bioavailability | Oral immediate-release: 80-90%; bioavailability is reduced by food; sodium bicarbonate formulation increases bioavailability via gastric pH elevation |
| Onset of Action | Oral: 2.5-3 hours for maximal acid suppression; significant effect within 1 hour |
| Duration of Action | Up to 24 hours after single dose; acid suppression persists for 2-3 days after discontinuation |
20 mg orally once daily before a meal for 14 days for frequent heartburn; 20 mg orally once daily for up to 8 weeks for erosive esophagitis healing; 20 mg orally once daily for maintenance of healed erosive esophagitis (up to 12 months).
| Dosage form | CAPSULE |
| 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 daily dose is 20 mg. |
| Liver impairment | For mild to moderate hepatic impairment (Child-Pugh A or B): no dose adjustment. For severe hepatic impairment (Child-Pugh C): maximum daily dose is 20 mg. |
| Pediatric use | For children 2 years and older: weight-based dosing. For erosive esophagitis: 5 mg (5-15 kg), 10 mg (16-30 kg), 20 mg (>30 kg) once daily for up to 8 weeks. For children 1 year and older: 2.5 mg (3-5 kg), 5 mg (6-15 kg), 10 mg (16-30 kg), 20 mg (>30 kg) once daily for up to 8 weeks for GERD. |
| Geriatric use | No specific dose adjustment required, but consider lower starting doses (20 mg daily) due to potential for decreased renal function and increased risk of adverse effects such as Clostridioides difficile infection and osteoporosis-related fractures. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ZEGERID OTC (ZEGERID OTC).
| Breastfeeding | Omeprazole is excreted in human milk; the milk-to-plasma ratio (M/P) is approximately 0.2. The estimated infant dose is less than 7% of the maternal weight-adjusted dose. Use with caution, especially in preterm infants due to potential gastric acid suppression. |
| Teratogenic Risk | FDA Pregnancy Category C. First trimester: Limited human data; animal studies showed no teratogenicity at doses up to 2.5 times the human dose. Second and third trimesters: No known fetal risk; omeprazole crosses the placenta but no increased malformation risk in retrospective studies. |
■ FDA Black Box Warning
No black box warning.
| Serious Effects |
["Hypersensitivity to omeprazole or any formulation component","Concomitant use with rilpivirine-containing products"]
| Precautions | ["Increased risk of Clostridioides difficile infection","Bone fracture risk with long-term use","Hypomagnesemia","Vitamin B12 deficiency","Acute interstitial nephritis","Cutaneous lupus erythematosus","Cyanocobalamin deficiency","Interaction with clopidogrel (reduced efficacy)","Interaction with methotrexate (increased toxicity)"] |
Loading safety data…
| Fetal Monitoring |
| No specific monitoring required beyond standard prenatal care. Monitor maternal symptoms of GERD for efficacy. No fetal monitoring indicated. |
| Fertility Effects | Animal studies at high doses showed reversible impairment of fertility; no human data on fertility effects. Generally considered unlikely to impair fertility at therapeutic doses. |