Lyophilized Omeprazole Sodium Powder for Injection 40mg

• Customization: Available
• Application: Injections
• Usage Mode: IV Injection
• Model NO.: Omeprazole 40mg
• Suitable for: Elderly, Children, Adult
• State: Solid
• Shape: Powder
• Type: Organic Chemicals
• Pharmaceutical Technology: Chemical Synthesis
• Transport Package: Carton Box
• Specification: 40mg
• Origin: China
• Production Capacity: 10000000 Boxes/Month

Product Description

1 PRODUCT NAME
OMEPRAZOLE Sodium for Injection 40 mg

 2 QUALITATIVE AND QUANTITATIVE COMPOSITION
Omeprazole 40 mg for intravenous injection

3 PHARMACEUTICAL FORM
Omeprazole Injection 40 mg. Each vial contains a white to off-white lyophilised powder consisting of omeprazole sodium 42.6 mg, equivalent to omeprazole 40 mg, which is intended to be reconstituted with the diluent provided. No other injection solution should be used. The cap is aluminium with a white coloured plastic flip-off lid.

4 CLINICAL PARTICULARS
4.1 Therapeutic indications
Omeprazole Injection 40 mg is indicated primarily for the treatment of Zollinger-Ellison syndrome, and may also be used for the treatment of gastric ulcer, duodenal ulcer and reflux oesophagitis.
4.2 Dose and method of administration
In patients with duodenal ulcer, gastric ulcer or reflux oesophagitis where oral medication is inappropriate, Omeprazole Injection 40 mg once daily is recommended.
In patients with Zollinger-Ellison syndrome the recommended initial dose of omeprazole given intravenously is 60 mg daily. Higher daily doses may be required and the dose should be adjusted individually. When doses exceed 60 mg daily, the dose should be divided and given twice daily.

Impaired Renal Function
Dose adjustment is not needed in patients with impaired renal function.

Impaired Hepatic Function
As plasma half-life of omeprazole is increased in patients with impaired hepatic function a daily dose of 10 - 20 mg may be sufficient.
Elderly
Dose adjustment is not needed in the elderly.
Children
There is limited experience with omeprazole IV in children.
Method of Administration
Omeprazole Injection 40 mg should be given as a slow intravenous injection. The solution for IV injection is obtained by adding to the vial 10 mL of the solvent provided. (No other solvent should be used). Discoloration may occur if incorrect reconstitution technique is used. For practical information about the reconstitution see the package insert. After reconstitution the injection should be given slowly over a period of at least 2.5 minutes at a maximum rate of 4 ml per minute. The solution should be used within 4 hours of reconstitution.

4.3 Contraindications
Known hypersensitivity to omeprazole.
4.4 Special warnings and precautions for use
In the presence of any alarm symptom (e.g. significant unintentional weight loss, recurrent vomiting, dysphagia, haematemesis or melena) and when gastric ulcer is suspected or present, the possibility of malignancy should be excluded as treatment may alleviate symptoms and delay diagnosis.
4.5 Interaction with other medicines and other forms of interaction Effects of omeprazole on the pharmacokinetics of other medicines
Omeprazole has been reported to interact with some antiretroviral medicines. The clinical importance and the mechanisms behind these interactions are not always known. Increased gastric pH during omeprazole treatment may change the absorption of the antiretroviral medicine. Other possible interaction mechanisms are via CYP 2C19. For some antiretroviral medicines, such as atazanavir and nelfinavir, decreased serum levels have been reported when given together with omeprazole. Concomitant administration with omeprazole and medicines such as atazanavir and nelfinavir is therefore not recommended.
Citalopram / Escitalopram
Co-administration of omeprazole (20 mg) with citalopram (20 mg single dose) doubles the AUC of the S-isomer of citalopram, but the R-isomer of citalopram is not affected. A reduction in the dose of citalopram may be necessary based on clinical judgement. For patients taking omeprazole, the citalopram dose should not exceed the maximum dose of 20 mg/day.

Co-administration of omeprazole (30 mg) with escitalopram (20 mg single dose) increased the plasma levels (approximately 50%) and terminal half-life (31%) of escitalopram. A reduction in the dose of escitalopram may be necessary based on clinical judgement.
Digoxin Concomitant treatment with omeprazole (20 mg daily) and digoxin in healthy subjects increased the bioavailability of digoxin by 10% (up to 30% in two out of ten subjects).
Clopidogrel Results from studies in healthy subjects have shown a pharmacokinetic/pharmacodynamic interaction between clopidogrel (300 mg loading dose/75 mg daily maintenance dose) and omeprazole (80 mg p.o. daily, i.e. four times the recommended dose) resulting in decreased exposure to the active metabolite of clopidogrel by an average of 46%, and resulting in decreased maximum inhibition of (ADP induced) platelet aggregation by an average of 16%.
It is, however, uncertain to what extent this interaction is clinically important. One prospective, randomised (but incomplete) study (in over 3760 patients comparing placebo with omeprazole 20 mg in patients treated with clopidogrel and ASA) and non-randomised, post-hoc analyses of data from large, prospective, randomised clinical outcome studies (in over 47000 patients) did not show any evidence of an increased risk for adverse cardiovascular outcome when clopidogrel and PPIs, including omeprazole, were given concomitantly.
Results from a number of observational studies are inconsistent with regard to increased risk or no increased risk for CV thromboembolic events when clopidogrel is given together with a PPI.
When clopidogrel was given together with a fixed dose combination of esomeprazole 20 mg + ASA 81 mg compared to clopidogrel alone in a study in healthy subjects there was a decreased exposure by almost 40% of the active metabolite of clopidogrel. However, the maximum levels of inhibition of (ADP induced) platelet aggregation in these subjects were the same in the clopidogrel and the clopidogrel + the combined (esomeprazole + ASA) product groups, likely due to the concomitant administration of low dose ASA.
Other active substances
The absorption of erlotinib, ketoconazole and itraconazole is significantly reduced and thus clinical efficacy may be impaired. For posaconazole and erlotinib concomitant use should be avoided.
Active substances metabolised by CYP2C19
Omeprazole inhibits CYP2C19, the major omeprazole metabolising enzyme. Thus, the metabolism of concomitant medicines also metabolised by CYP2C19, such as phenytoin, warfarin (R-warfarin) or other vitamin K antagonists and cilostazol, may be delayed.
Monitoring of patients receiving phenytoin is recommended and a reduction of the phenytoin dose may be necessary. However concomitant treatment with omeprazole capsules 20 mg, daily did not change the blood concentration of phenytoin in patients on continuous treatment with this medicine.
In patients receiving warfarin or other vitamin K antagonists, monitoring of INR is recommended and a reduction of the warfarin (or other vitamin K antagonist) dose may be necessary. Concomitant treatment with omeprazole 20 mg orally, daily did, however, not change coagulation time in patients on continuous treatment with warfarin.
Cilostazol
Omeprazole, given in doses of 40 mg to healthy subjects in a cross-over study, increased Cmax and AUC for cilostazol by 18% and 26% respectively, and one of its active metabolites by 29% and 69% respectively.
Other
Omeprazole is partly metabolised also by CYP3A4, but omeprazole does not inhibit this enzyme. Thus, omeprazole does not affect the metabolism of medicines metabolised by CYP3A4, such as cyclosporin, quinidine, oestradiol, erythromycin. However, omeprazole has been shown to induce CYP1A2-mediated metabolism of clozapine. Close monitoring of plasma clozapine levels is recommended.
Results from a range of interaction studies with omeprazole versus other medicines demonstrate that omeprazole, 20-40 mg daily, has no significant influence on any other CYP enzymes relevant for medicine metabolism, as shown by the lack of metabolic interaction with substrates for CYP1A2 (such as theophylline), CYP2C9 (such as S-warfarin, piroxicam, diclofenac, naproxen), CYP2E1 (such as ethanol). However, omeprazole has been shown to induce CYP1A2-mediated metabolism of clozapine. Close monitoring of plasma clozapine levels is recommended.

4.6 Fertility, pregnancy and lactation
Pregnancy
Results from three prospective epidemiological studies indicate no adverse effects of omeprazole on pregnancy or on the health of the foetus/newborn child. Omeprazole can be used during pregnancy.
Breast feeding
Omeprazole is excreted in breast milk but is not likely to influence the child when therapeutic doses are used.

4.7 Effects on ability to drive and use machines
Omeprazole is not likely to affect the ability to drive or use machines.

4.8 Undesirable effects
Omeprazole is well tolerated and adverse reactions have generally been mild and reversible. The following events have been reported as adverse events in clinical trials or reported from routine use, but in many cases a relationship to treatment with omeprazole has not been established.
The following definitions of frequencies are used:
Common ≥1/100
Uncommon ≥1/1,000 and <1/1,00
Rare     <1/1,000

4.9 Overdose
Omeprazole IV doses of up to 270 mg on a single day and up to 650 mg over a three-day period have been given in clinical trials without any dose-related adverse reactions.

5. Special precautions for storage
Omeprazole for Injection must be dissolved in the 10 ml of diluent provided.
Chemical and physical in-use stability has been demonstrated for 4 hours after reconstitution.
From a microbiological point of view, the product should be used immediately, unless reconstitution has taken place in controlled and validated aseptic conditions. The solution can be handled at normal indoor light without special precaution. Any unused portion should be discarded.