Treatment of frequent heartburn that occurs 2 or more times per week.
As alternate-day therapy in maintaining ulcer or GERD remission rates during long-term treatment after healing during a short course of therapy; treatment of GERD-related laryngitis symptoms in patients who have not responded to antireflux measures alone; treatment of GERD in infants and children; in combination with antibiotics (eg, amoxicillin, clarithromycin) for eradication of H. pylori in children; to improve enzyme absorption in cystic fibrosis patients with intestinal
Active Duodenal Ulcer
Adults: PO 20 mg/day for 4 to 8 wk.
Adults: PO 40 mg once daily for 4 to 8 wk.
GERD and Maintenance of Healing of Erosive Esophagitis
Children 1 y of age and older: PO Weighing 5 to less than 10 kg, the dosage is 5 mg daily. Weighing 10 kg to less than 20 kg, the dosage is 10 mg daily.
Weighing 20 kg or more, the dosage is 20 mg daily.
GERD With Erosive Esophagitis
Adults: PO 20 mg/day for 4 to 8 wk. For maintenance treatment, give 20 mg/day.
GERD Without Esophageal Lesions
Adults: PO 20 mg daily for up to 4 wk.
Adults: PO 20 mg daily for 14 days. The 14-day course may be repeated every 4 mo.
Adults (triple therapy): PO Omeprazole 20 mg plus clarithromycin 500 mg plus amoxicillin 1,000 mg each given 2 times daily for 10 days; continue omeprazole 20 mg/day for an additional 18 days if an ulcer is present at start of therapy.
Adults (dual therapy): PO Omeprazole 40 mg once daily plus clarithromycin 500 mg 3 times daily for 14 days; continue omeprazole 20 mg/day for an additional 14 days if an ulcer is present at start of therapy.
Pathologic Hypersecretory Conditions
Adults: PO Initial dosage, 60 mg/day. Dosages up to 120 mg 3 times daily have been given. Divide daily doses of more than 80 mg.
|•||Administer on an empty stomach at least 1 h before a meal. Capsules and tablets should not be crushed or chewed.|
|•||For patients who have difficulty swallowing capsules, the contents of a delayed-release capsule can be added to a tablespoon of applesauce in a bowl. The pellets should be mixed with the applesauce and swallowed immediately with a glass of cool water. The applesauce should be soft enough to swallow without chewing and should not be heated. The omeprazole pellets should not be chewed or crushed. Do not store the pellets/applesauce mixture for future use.|
|•||Administer delayed-release suspension by emptying contents of a 2.5 mg packet into 5 mL of water or by emptying contents of a 10 mg packet into 15 mL of water. Stir and leave for 2 to 3 min to thicken. Stir and drink within 30 min. If any material remains after drinking, add more water, stir and drink immediately.|
|•||For patients with a nasogastric (NG) or gastric tube, add 5 mL of water to a catheter-tipped syringe and then add the contents of a 2.5 mg packet (or 15 mL of water for the 10 mg packet). Only use a catheter-tipped syringe when administering omeprazole through an NG or gastric tube. Immediately shake the syringe and allow 2 to 3 min to thicken. Shake the syringe and inject contents through the nasogastric or gastric tube into the stomach within 30 min, using a French size 6 or larger. Refill the syringe with an equal amount of water, shake, and flush any remaining contents from the NG or gastric tube into the stomach.|
Suppresses gastric acid secretion by blocking acid (proton) pump within gastric parietal cell.
Hypersensitivity to substituted benzimidazoles or to any component of the formulation.
Use Cautiously in:
|•||Liver disease (dosage reduction may be necessary).|
|•||Geri: Increased risk of hip fractures in patients using high-doses for > 1 year.|
|•||Bartter’s syndrome, hypokalemia, and respiratory alkalosis (Zegerid only).|
|•||Pregnancy, lactation, or children <2 yr (safety not established).|
CV: Angina or chest pain, bradycardia, elevated BP, palpitations, peripheral edema, tachycardia (postmarketing).
CNS: Headache (7%); dizziness (2%); asthenia (1%); abnormal dreams, aggression, agitation, anxiety, apathy, confusion, depression, fatigue, hallucinations, insomnia, malaise, nervousness, paresthesia, sleep disturbances, somnolence, tremors, vertigo (postmarketing).
DERM: Rash (2%); alopecia, dry skin, erythema multiforme, hyperhidrosis, petechiae, photosensitivity, pruritus, purpura, skin inflammation, Stevens-Johnson syndrome, TEN, urticaria (postmarketing).
EENT: Anterior ischemic optic neuropathy, blurred vision, double vision, dry eye syndrome, ocular irritation, optic atrophy, optic neuritis, pharyngeal pain, taste perversion, tinnitus (postmarketing).
GI: Abdominal pain (5%); diarrhea, nausea (4%); flatulence, vomiting (3%); acid regurgitation, constipation (2%); abdominal swelling, anorexia, dry mouth, esophageal candidiasis, fecal discoloration, gastric fundic gland polyps, gastroduodenal carcinoids, irritable colon, mucosal atrophy of the tongue, pancreatitis, stomatitis (postmarketing).
GU: Elevated serum creatinine, glucosuria, gynecomastia, hematuria, interstitial nephritis, microscopic pyuria, proteinuria, testicular pain, urinary frequency, UTI (postmarketing).
HEPA: Cholestatic disease, elevated LFTs (alkaline phosphatase, bilirubin, ALT, AST, GGT), hepatic encephalopathy, hepatic failure (some fatal), hepatocellular disease, jaundice, liver necrosis, mixed hepatitis (postmarketing).
HEMA/LYMPH: Agranulocytosis, anemia, hemolytic anemia, leukocytosis, leukopenia, neutropenia, pancytopenia, thrombocytopenia (postmarketing).
HYPERSEN: Anaphylactic shock, anaphylaxis, angioedema, bronchospasm, interstitial nephritis, urticaria (postmarketing).
M/N: Hypoglycemia, hypomagnesemia, hyponatremia, weight gain (postmarketing).
MUSC: Back pain (1%); bone fracture, joint pain, leg pain, muscle cramps, muscle weakness, myalgia (postmarketing).
RESP: Upper respiratory tract infection (2%); cough (1%); epistaxis (postmarketing).
OTHER: Fever (children 1 to 2 y of age, 33%); pain (postmarketing).
The inhibition of gastric acid secretion may interfere with the absorption of ampicillin esters in which gastric pH is an important determinant of bioavailability. Temporary cessation of omeprazole treatment may be required in order to achieve the appropriate clinical response to ampicillin.
Atazanavir, nelfinavir, ritonavir
Plasma concentrations may be reduced by omeprazole, decreasing the efficacy. Coadministration with omeprazole is not recommended.
Azole antifungal agents (eg, itraconazole, ketoconazole)
The bioavailability of certain azole antifungals may be decreased. Avoid coadministration if possible. If concurrent use cannot be avoided, consider instructing the patient to take with an acidic beverage (eg, Coca-Cola ) to help increase azole antifungal absorption.
Benzodiazepines (eg, diazepam)
Cl of benzodiazepines may be decreased. Monitor for increased CNS impairment and reduce the benzodiazepine dosage or increase the dosing interval if needed. Benzodiazepines not metabolized by oxidation (eg, lorazepam) may not interact.
Omeprazole may decrease GI absorption of calcium salts. Closely monitor the clinical response to calcium salts. Larger dosages of calcium salts may be needed for patients taking long-term omeprazole.
Carbamazepine plasma concentrations may be elevated, increasing the risk of toxicity. Additional carbamazepine concentration and clinical monitoring is warranted. Adjust the carbamazepine dose as needed when starting or stopping omeprazole.
Plasma levels may be increased by omeprazole, increasing the therapeutic effects and adverse reactions. Consider dosage adjustment of cilostazol from 100 to 50 mg twice daily. Monitor tacrolimus trough concentrations when omeprazole is started or stopped. Adjust the tacrolimus dose as needed.
Omeprazole and clarithromycin plasma concentrations may be elevated. Based upon available data, no special action is needed.
Controlled studies are needed to determine the magnitude of this interaction with each proton pump inhibitor (PPI) and clopidogrel. The antiplatelet activity of clopidogrel may be decreased by omeprazole. Omeprazole may interfere with the metabolic (CYP2C19) conversion of clopidogrel to its active metabolite. If omeprazole is clearly indicated in a patient receiving clopidogrel, use with caution. An antacid or H2 receptor antagonist (eg, ranitidine) may be a safer alternative.
Clozapine plasma concentrations and pharmacologic effects may be increased. Clozapine toxicity may occur. Close clinical and laboratory monitoring is warranted. Adjust the clozapine dose as needed.
Dasatinib, erlotinib, nilotinib
Omeprazole may interfere with the absorption of these agents. Plasma concentration and pharmacologic effects of these agents may be decreased. Avoid coadministration with omeprazole.
Coadministration may increase serum digoxin concentrations. The magnitude of this change would not be expected to be clinically important in most patients.
The neuropsychiatric toxicity of disulfiram may be increased. The clinical importance of this interaction is not known. If an interaction is suspected, it may be necessary to discontinue both drugs.
Omeprazole plasma concentrations may be elevated, increasing the risk of adverse reactions. Monitor for an increase in adverse reactions.
Administration of omeprazole with applesauce may decrease the omeprazole Cmax with a change in the AUC. The clinical importance is unknown. It is recommended that omeprazole capsules be administered before meals.
Ginkgo biloba , St. John’s wort
Omeprazole plasma concentrations may be reduced, decreasing the therapeutic effect. Avoid concurrent use.
Hydantoins (eg, phenytoin)
Decreased plasma Cl and increased phenytoin half-life. Serum hydantoin levels may be elevated, increasing the pharmacologic effects and risk of toxicity. Observe the patient for adverse effects and monitor phenytoin serum concentrations. Adjust the hydantoin dose as needed.
The inhibition of gastric acid secretion may interfere with the absorption of drugs in which gastric pH is an important determinant of bioavailability. Temporary cessation of omeprazole treatment may be required in order to achieve the appropriate clinical response to oral iron. If stopping omeprazole is not an option, parenteral iron may be a suitable alternative.
Omeprazole may decrease the renal elimination of methotrexate, increasing methotrexate concentrations and the risk of toxicity. Closely monitor methotrexate concentrations and monitor for signs of methotrexate toxicity. Longer duration of leucovorin rescue, systemic hydration, and urinary alkalinization may be required for high-dose methotrexate. Consider discontinuing or suspending omeprazole.
Mycophenolate plasma concentrations and pharmacologic effects may be decreased. Larger mycophenolate doses may be needed during coadministration of omeprazole. Monitor the clinical response and adjust the mycophenolate dose as needed.
Although no interaction with propranolol and omeprazole has been reported, interactions have been reported with other drugs metabolized by the CYP-450 system. Clinical and laboratory monitoring of propranolol is warranted. Adjust the propranolol dose as needed.
Enteric-coated salicylates may dissolve more rapidly, increasing gastric adverse effects. Patients at risk of serious gastric disorders due to the release of salicylates in the stomach should avoid concurrent use of these agents.
Plasma concentrations may be elevated by omeprazole, increasing the risk of adverse reactions. Consider saquinavir dose reduction.
The rate of theophylline absorption from slow-release forms of theophylline may be increased. In addition, interactions have been reported with other drugs metabolized by the CYP-450 system. Clinical and laboratory monitoring is warranted. Adjust the theophylline dose as needed.
An increase in the release of tolterodine from the ER dosage form may occur as a result of the increase in gastric pH associated with PPI administration. Plasma concentrations of tolterodine and its active metabolite may be elevated, increasing the pharmacologic effects and risk of adverse reactions. Monitor the clinical response and for adverse reactions. Adjust the tolterodine dose as needed.
Omeprazole plasma concentrations may be elevated, which may necessitate dosage adjustments in patients with Zollinger-Ellison syndrome.
Increased INR and PT, which may lead to abnormal bleeding and increase the risk of death. Monitor anticoagulant parameters when starting or stopping omeprazole and adjust the warfarin dose as needed.
Therapeutic Classification: antiulcer agents
Pharmacologic Classification: proton pump inhibitors
Absorption: Rapidly absorbed following oral administration; immediate release formulation contains bicarbonate to prevent acid degradation.
Distribution: Good distribution into gastric parietal cells.
Protein Binding: 95%.
Metabolism/Excretion: Extensively metabolized by the liver.
Half-life: 0.5–1 hr (increased in liver disease to 3 hr).
|ORAL||WITHIN 1 HOUR||WITHIN 2 HOUR||72-96 HOUR|
|ORAL IMMEDIATE RELEASE||RAPID||30MINUTE||24 HOUR|