OTC labeling: Short-term treatment of frequent, uncomplicated heartburn occurring
2 days/week
Zegerid™: Also contraindicated with metabolic alkalosis and hypocalcemia (due to sodium bicarbonate content)
1% to 10%:
Central nervous system: Headache (7%), dizziness (2%)
Dermatologic: Rash (2%)
Gastrointestinal: Diarrhea (3%), abdominal pain (2%), nausea (2%), vomiting (2%), constipation (1%), taste perversion (<1% to 15%)
Neuromuscular & skeletal: Weakness (1%), back pain (1%)
Respiratory: Upper respiratory infection (2%), cough (1%)
<1%: Abdominal swelling, abnormal dreams, aggression, agranulocytosis, allergic reactions, alopecia, anaphylaxis, anemia, angina, angioedema, anorexia, anxiety, apathy, atrophic gastritis, benign gastric polyps, blurred vision, bradycardia, jaundice, confusion, depression, diaphoresis, double vision, dry mouth, dry skin, epistaxis, erythema multiforme, esophageal candidiasis, fatigue, fecal discoloration, fever, flatulence, glycosuria, gynecomastia, hallucinations, hematuria, hemifacial dysesthesia, hemolytic anemia, hepatic encephalopathy, hepatic failure, hepatic necrosis, hypertension, hypoglycemia, hyponatremia, insomnia, interstitial nephritis, irritable colon, joint pain, leg pain, leukocytosis; liver disease (hepatocellular, cholestatic, mixed); malaise, microscopic pyuria, mucosal atrophy (tongue), muscle cramps, muscle weakness, myalgia, nervousness, neutropenia, ocular irritation, pain, palpitation, pancreatitis, pancytopenia, paresthesia, peripheral edema, pharyngeal pain, phosphatase, proteinuria, pruritus, psychic disturbance, rash, serum alkaline increased, serum creatinine increased, serum transaminases increased, skin inflammation, somnolence, Stevens-Johnson syndrome, tachycardia, testicular pain, thrombocytopenia, tinnitus, toxic epidermal necrolysis, tremor, urinary frequency, urinary tract infection, urticaria, vertigo, weight gain
Zegerid™: Also consider sodium bicarbonate overdose.
Benzodiazepines metabolized by oxidation (eg, diazepam, midazolam, triazolam): Esomeprazole and omeprazole may increase levels of benzodiazepines metabolized by oxidation.
Carbamazepine: Esomeprazole and omeprazole may increase carbamazepine levels.
CYP2C8/9 substrates: Omeprazole may increase the levels/effects of CYP2C8/9 substrates. Example substrates include amiodarone, fluoxetine, glimepiride, glipizide, nateglinide, phenytoin, pioglitazone, rosiglitazone, sertraline, and warfarin.
CYP2C19 inducers: May decrease the levels/effects of omeprazole. Example inducers include aminoglutethimide, carbamazepine, phenytoin, and rifampin.
CYP2C19 substrates: Omeprazole may increase the levels/effects of CYP2C19 substrates. Example substrates include citalopram, diazepam, methsuximide, phenytoin, propranolol, and sertraline.
Itraconazole and ketoconazole: Proton pump inhibitors may decrease the absorption of itraconazole and ketoconazole.
Phenytoin: Elimination of phenytoin may be prolonged; monitor. Phenytoin may decrease omeprazole levels/effects.
Protease inhibitors: Proton pump inhibitors may decrease absorption of some protease inhibitors (atazanavir and indinavir).
Warfarin: Elimination of warfarin may be prolonged; monitor.
Ethanol: Avoid ethanol (may cause gastric mucosal irritation).
Food: Food delays absorption. When Zegerid™ is given 1 hour after a meal, absorption is reduced.
Herb/Nutraceutical: St John's wort may decrease omeprazole levels.
Onset of action: Antisecretory: ~1 hour
Peak effect: 2 hours
Duration: 72 hours
Protein binding: 95%
Metabolism: Extensively hepatic to inactive metabolites
Bioavailability: Oral: 30% to 40%; increased in Asian patients and with hepatic dysfunction
Half-life elimination: 0.5-1 hour
Excretion: Urine (77% as metabolites, very small amount as unchanged drug); feces
Children
2 years: GERD or other acid-related disorders:
<20 kg: 10 mg once daily
20 kg: 20 mg once daily
Adults:
Active duodenal ulcer: 20 mg/day for 4-8 weeks
Gastric ulcers: 40 mg/day for 4-8 weeks
Symptomatic GERD: 20 mg/day for up to 4 weeks
Erosive esophagitis: 20 mg/day for 4-8 weeks
Helicobacter pylori eradication: Dose varies with regimen: 20 mg once daily or 40 mg/day as single dose or in 2 divided doses; requires combination therapy with antibiotics
Pathological hypersecretory conditions: Initial: 60 mg once daily; doses up to 120 mg 3 times/day have been administered; administer daily doses >80 mg in divided doses
Frequent heartburn (OTC labeling): 20 mg/day for 14 days; treatment may be repeated after 4 months if needed
Dosage adjustment in hepatic impairment: Specific guidelines are not available; bioavailability is increased with chronic liver disease
Capsule: Should be swallowed whole; do not chew, crush, or open. Best if taken before breakfast. May be opened and contents added to applesauce. Administration via NG tube should be in an acidic juice.
Powder for oral suspension (Zegerid™): Administer 1 hour before a meal. Mix with 2 tablespoons of water; stir well and drink immediately. Rinse cup with water and drink.
Should be taken on an empty stomach; best if taken before breakfast.
Zegerid™: Take 1 hour before a meal; contains sodium bicarbonate 1680 mg (20 mEq), equivalent to sodium 460 mg (20 mEq) per dose
DiGiancinto JL, Olsen KM, Bergman KL, et al, "Stability of Suspension Formulations of Lansoprazole and Omeprazole Stored in Amber-Colored Plastic Oral Syringes," Ann Pharmacother , 2000, 34:600-5.
Quercia R, Fan C, Liu X, et al, "Stability of Omeprazole in an Extemporaneously Prepared Oral Liquid," Am J Health Syst Pharm , 1997, 54:1833-6.
Sharma V, "Comparison of 24-hour Intragastric pH Using Four Liquid Formulations of Lansoprazole and Omeprazole," Am J Health Syst Pharm , 1999, 56(Suppl 4):S18-21.
Capsule, delayed release: 10 mg, 20 mg
Prilosec®: 10 mg, 20 mg, 40 mg
Prilosec OTC™: 20 mg
Powder for oral suspension (Zegerid™): 20 mEq/packet (30s) [contains sodium bicarbonate 1680 mg, equivalent to sodium 460 mg]
DiGiancinto JL, Olsen KM, Bergman KL, et al, "Stability of Suspension Formulations of Lansoprazole and Omeprazole Stored in Amber-Colored Plastic Oral Syringes," Ann Pharmacother , 2000, 34:600-5.
Quercia R, Fan C, Liu X, et al, "Stability of Omeprazole in an Extemporaneously Prepared Oral Liquid," Am J Health Syst Pharm , 1997, 54:1833-6.
Sharma V, "Comparison of 24-hour Intragastric pH Using Four Liquid Formulations of Lansoprazole and Omeprazole," Am J Health Syst Pharm , 1999, 56(Suppl 4):S18-21.
Extemporaneous preparation for NG administration (Prilosec®): The manufacturer recommends the use of an acidic juice for preparation to administer via nasogastric (NG) tube. Alternative methods have been described as follows. NG tube administration for the prevention of stress-related mucosal damage in ventilated, critically-ill patients. The manufacturer makes no judgment regarding the safety or efficacy of these practices.
The contents of one or two 20 mg omeprazole capsules were poured into a syringe; 10-20 mL of an 8.4% sodium bicarbonate solution was withdrawn in the syringe; 30 minutes were allowed for the enteric-coated omeprazole granules to break down. The resulting milky substance was shaken prior to administration. The NG tube was then flushed with 5-10 mL of water then clamped for at least 1 hour. Patients received omeprazole 40 mg once, then 40 mg 6-8 hours later, then 20 mg once daily using this technique.
Another study used a different technique. The omeprazole capsule (20 mg or 40 mg) was opened; then the intact granules were poured into a container holding 30 mL of water. With the plunger removed, 1 /3 to 1 /2 of the granules were then poured into a 30 mL syringe which was attached to a nasogastric tube (NG). The plunger was replaced with 1 cm of air between the granules and the plunger top while the plunger was depressed. This process was repeated until all the granules were flushed, then a final 15 mL of water was flushed through the tube. Patients who received omeprazole 40 mg in this manner had a more predictable increase in intragastric pH than patients who received omeprazole 20 mg.
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