Gufic Biosciences


Full Prescribing Info
Omeprazole sodium.
Each combipack contains: Omeprazole sodium eq. to Omeprazole, BP 40 mg (Suitably Buffered), and
Sterile Water for Injection, BP 10 mL.
Omeprazole is a proton pump inhibitor and gastric secretory agent used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD) and Zollinger-Ellison syndrome.
Pharmacology: Pharrmacodynamics: Omeprazole is a weak base and is concentrated and converted to the active form in the highly acidic environment of the intracellular canaliculi within the parietal cell, where it inhibits the enzyme H+, K+-ATPase, the acid pump. This effect on the final step of the gastric acid formation process is dose-dependent and provides for highly effective inhibition of both basal acid secretion and stimulated acid secretion, irrespective of the stimulus. All pharmacodynamic effects observed can be explained by the effect of omeprazole on acid secretion.
Pharrmacokinetics: Omeprazole is rapidly but variably absorbed after oral doses. Absorption is not significantly affected by food. Omeprazole is acid-labile and the pharmacokinetics of the various formulations developed to improve oral bioavailability may vary. The absorption of omeprazole also appears to be dose-dependent; increasing the dosage above 40 mg has been reported to increase the plasma concentrations in a non-linear fashion because of saturable first-pass hepatic metabolism. In addition, bioavailability is higher after long-term use. Bioavailability of omeprazole may be increased in elderly patients, in some ethnic groups such as Chinese and in patients with hepatic impairment, but is not markedly affected in patients with renal impairment. On absorption, omeprazole is almost completely metabolised in the liver, primarily by the cytochromeP450 isoenzyme CYP2C19 to form hydroxy-omeprazole and to a small extent by CYP3A4 to form omeprazole sulfone. The metabolites are inactive and are excreted mostly in the urine and to a lesser extent in bile. The elimination half-life from plasma is reported to be about 0.5 to 3 hours. Omeprazole is about 95% bound to plasma proteins.
Duodenal Ulcer: Gastric Ulcer; Reflux esophagitis and esophageal ulceration; Zollinger-Ellison Syndrome; Resistant Ulcer; Eradication of Helicobacter pylori in combination with antibiotics.
Dosage/Direction for Use
Omeprazole for Injection to be given by intravenous injection over 5 minutes or by intravenous infusion over 20-30 minutes, prophylaxis of acid aspiration: 40 mg completed 1 hour before surgery.
Benign gastric ulcer, duodenal ulcer and gastroesophageal reflux: 40 mg once daily until oral administration. Possible severe peptic ulcer bleeding [unlicensed indication]: initial intravenous infusion of 80 mg then by continuous intravenous infusion, 8 mg/hour for 72 hours.
In patients who are unsuited to receive oral therapy, omeprazole sodium may be given on a short-term basis by intravenous infusion: in a usual dose equivalent to 40 mg of the base over a period of 20 to 30 minutes in 100 mL of sodium chloride 0.9% or glucose 5%. It may also be given by slow intravenous injection. Higher intravenous doses have been given to patients with Zollinger-Ellison syndrome.
For parenteral dosage in children, an intravenous dose of 500 micrograms/kg (to a maximum of 20 mg) once daily in children aged 1 month to 12 years. This may be increased to 2 mg/kg (to a maximum of 40 mg) once daily if needed.
Mode of Administration: Intravenous use only.
Reconstitution: Omeprazole for Injection 40 mg should be reconstituted with the solvent provided.
For IV infusion Omeprazole for Injection 40 mg should be reconstituted with 100 mL of sodium chloride 0.9% or glucose 5%.
There is no sufficient information available on deliberate over dosage with Omeprazole.
Hypersensitivity to any component of the formulation and other substituted benzimidazoles (rabeprazole, esomeprazole).
Special Precautions
Gastritis: Atrophic gastritis has been noted occasionally in gastric corpus biopsies from patients treated long-term with omeprazole and esomeprazole.
Hepatic effects: In patients with various degrees/types of hepatic disease, the area under the curve (AUC) was prolonged (lansoprazole, esomeprazole, rabeprazole, pantoprazole), half-life was prolonged (lansoprazole, omeprazole, rabeprazole, pantoprazole), increased bioavailability was observed (omeprazole), decreased clearance with rabeprazole and increased maximum pantoprazole concentrations.
Gastric malignancy: Symptomatic response to therapy with proton pump inhibitors does not preclude gastric malignancy.
Use in Pregnancy: Category C (omeprazole); Category B (lansoprazole, rabeprazole, pantoprazole, esomeprazole).
Use in Lactation: Omeprazole has been measured in the breast milk. Because of the potential for serious adverse reactions in breast-feeding infants, decide whether to discontinue breast-feeding or to discontinue the drug, taking into account the importance of the drug to the mother.
Use in Children: The safety and efficacy of omeprazole have not been established for pediatric patients younger than 2 years of age.
Use in Elderly: The elimination rate of omeprazole was somewhat decreased in the elderly and the bioavailability increased.
Use In Pregnancy & Lactation
Pregnancy: There is no adequate data on the safety of Omeprazole in pregnant woman.
Lactation: Omeprazole has been measured in the breast milk. Because of the potential for serious adverse reactions in breast-feeding infants, decide whether to discontinue breast-feeding or to discontinue the drug, taking into account the importance of the drug to the mother.
Adverse Reactions
Proton pump inhibitors are generally well tolerated and adverse effects are relatively infrequent. The adverse effects reported most often with omeprazole and other proton pump inhibitors have been headache, diarrhoea and skin rashes; they have sometimes been severe enough to require stopping treatment. Other effects include pruritus, dizziness, fatigue, constipation, nausea and vomiting, flatulence, abdominal pain, arthralgia and myalgia, urticaria and dry mouth. Isolated cases of photosensitivity, bullous eruption erythema multiforme, Stevens-Johnson syndrome and toxic epidermal necrolysis have occurred.
Hypersensitivity reactions, including fever, bronchospasm, angioedema and anaphylaxis have been reported. Effects on the CNS include occasional insomnia, somnolence and vertigo; reversible confusional states, agitation, depression and hallucinations have occurred in severely ill patients.
Raised liver enzymes and isolated cases of hepatitis, jaundice, hepatic failure and hepatic encephalopathy have been reported. Other adverse effects reported rarely include paraesthesia, blurred vision, alopecia, stomatitis, increased sweating, taste disturbances, peripheral oedema, malaise, hyponatraemia, blood disorders (including agranulocytosis, leucopenia and thrombocytopenia), gynaecomastia, impotence and interstitial nephritis. Proton pump inhibitors may increase the risk of gastrointestinal infections because of their acid suppressive effects.
Drug Interactions
Drugs that may be affected by proton pump inhibitors include azole antifungal agents (eg, itraconazole, ketoconazole), benzodiazepines, cilostazol, clarithromycin, digoxin, phenytoin, salicylates, sulfonylureas and warfarin.
Proton pump inhibitors cause a profound and long-lasting inhibition of gastric acid secretion; therefore, proton pump inhibitors may interfere with the absorption of drugs where gastric pH is an important determinant of bioavailability (eg, ketoconazole, ampicillin, iron salts, digoxin, cyanocobalamin).
P450 system: Drugs that may be affected by proton pump inhibitors include benzodiazepines, clarithromycin, cyclosporine, disulfiram, digoxin, azole antifungal agents, hydantoins, cilostazol, salicylates, sulfonylureas, and warfarin.
Drugs that affect proton pump inhibitors include clarithromycin and sucralfate.
Store at temperatures not exceeding 30°C. Protect from light.
ATC Classification
A02BC01 - omeprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
Powd for inj (vial) 40 mg (+10 mL diluent in amp) x 1's.
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