ZEGERID
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ZEGERID (ZEGERID).
Proton pump inhibitor that irreversibly inhibits the H+/K+ ATPase enzyme system at the secretory surface of gastric parietal cells, suppressing basal and stimulated gastric acid secretion.
| Metabolism | Primarily metabolized by CYP2C19 and CYP3A4 in the liver. |
| Excretion | Approximately 82% renal (as metabolites), 18% fecal (via bile); less than 1% unchanged in urine. |
| Half-life | 1.0–1.5 hours in plasma; however, the pharmacodynamic half-life is longer due to irreversible inhibition of H+/K+-ATPase; drug effect persists for 24 hours after single dose. |
| Protein binding | 96% bound to serum albumin and alpha1-acid glycoprotein. |
| Volume of Distribution | Approximately 0.15 L/kg; distributes primarily into extracellular fluid, with low penetration into CNS. |
| Bioavailability | Oral: approximately 50-55% (due to first-pass metabolism); intravenous: 100%. |
| Onset of Action | Oral: peak effect in 2.5–3 hours; clinical onset of acid suppression occurs within 1 hour. |
| Duration of Action | Acid suppression lasts up to 24 hours with once-daily dosing; maximal effect achieved after 4–5 days of repeated dosing. |
20 mg or 40 mg orally once daily before a meal.
| Dosage form | TABLET, CHEWABLE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment (CrCl <30 mL/min); use with caution. |
| Liver impairment | For mild to moderate hepatic impairment (Child-Pugh A or B): no dose adjustment. For severe hepatic impairment (Child-Pugh C): maximum dose 20 mg daily. |
| Pediatric use | Approved for children ≥2 years: weight ≥15 kg but <20 kg: 20 mg once daily; weight ≥20 kg: 40 mg once daily. Administer 30–60 minutes before a meal. |
| Geriatric use | No routine dose adjustment required. Consider lower starting dose (20 mg) due to potential decreased hepatic/renal function and increased risk of adverse effects. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ZEGERID (ZEGERID).
| Breastfeeding | Omeprazole is excreted in human breast milk. The milk-to-plasma (M/P) ratio is approximately 0.5. After a 40 mg oral dose, the estimated infant daily dose is about 0.4 mg (1.4% of maternal dose). Use with caution in nursing mothers; consider the developmental and health benefits of breastfeeding along with the mother's clinical need for Zegerid. Monitor infant for potential adverse effects such as diarrhea or constipation. |
| Teratogenic Risk | Pregnancy Category C. No adequate studies in pregnant women. In animal studies, omeprazole (the active ingredient) at doses up to 138 mg/kg/day (about 28 times the human dose) showed no evidence of teratogenicity. However, embryofetal toxicity (increased postimplantation loss, decreased fetal weight) occurred at maternally toxic doses. Use only if clearly needed and potential benefit justifies risk to fetus. First trimester: limited data suggest no increased risk of major malformations. Second/third trimester: no specific risks identified, but avoid prolonged use if possible. |
■ FDA Black Box Warning
No FDA boxed warning.
| Serious Effects |
["Hypersensitivity to omeprazole or any component of the formulation","Concomitant use with rilpivirine containing products"]
| Precautions | ["Gastric malignancy: Symptomatic response does not preclude presence of gastric malignancy.","Atrophic gastritis: May occur with long-term use.","Acute interstitial nephritis: Has been observed; discontinue if suspected.","Clostridioides difficile infection: May increase risk.","Bone fracture: Long-term use may increase risk of osteoporosis-related fractures.","Cyanocobalamin (Vitamin B12) deficiency: Long-term use may impair absorption.","Hypomagnesemia: Has been reported; monitor magnesium levels with prolonged use.","Interaction with methotrexate: May increase methotrexate levels.","Interaction with clopidogrel: Potential reduction of clopidogrel efficacy."] |
Loading safety data…
| Fetal Monitoring | No specific mandatory monitoring. Monitor for maternal gastrointestinal symptoms (diarrhea, constipation, abdominal pain) and potential Clostridium difficile infection. In prolonged use, assess for vitamin B12 deficiency and bone mineral density loss. In pregnancy, monitor for signs of maternal toxicity related to high doses. |
| Fertility Effects | Animal studies: Omeprazole at oral doses up to 138 mg/kg/day (about 28 times human dose) did not impair fertility or reproductive performance in rats. Human data: No evidence of adverse effects on human fertility. However, the potential for acid suppression to affect absorption of nutrients or drugs relevant to fertility should be considered. |