Each vial contains:
Lyophillized powder omeprazole sodium equivalent to omeprazole 40 mg
Omeprazole reversibly reduces gastric acid secretion by specifically inhibiting the gastric enzyme H+/K+-ATPase proton pump in the parietal cell. Chemically, it may be described as 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2pyridinyl)methyl]sulfinyl]-1H-benzimidazole. Omeprazole sodium is absorbed rapidly. Omeprazole sodium is 95% bound to plasma proteins. It is entirely metabolized, mainly in the liver, about 80% of the metabolites are excreted in urine and the remainder in feces.
Alternative therapy for the following conditions which cannot be treated effectively with oral medication: duodenal ulcer, gastric ulcer, reflux esophagitis and Zollinger-Ellison syndrome.
Omeprazole is contraindicated in patients with known hypersensitivity to the drug or any ingredient in the formulation.
Dosage and administration:
- Omeprazole intravenous should only be used where oral medication is inappropriate, e.g. in severely ill patients. Dose 40 mg, once daily.
- The dose used in the treatment of Zollinger-Ellison syndrome should be adjusted according to individual response.
- Dilute OMEPRAZOLE injection with 10 ml WFI, do not used another solvent. Inject over a period of not less than 2.5 minutes. Inject at a rate no greater than 4 ml/min.
- No dosage adjustment of OMEPRAZOLE injection is necessary in the impaired hepatic, renal function and elderly patients. There is no experience with omeprazole injection in children.
- OMEPRAZOLE injection should only be reconstituted by WFI, do not use other solvents. Discoloration may occur if incorrect reconstitution technique is used.
- With a syringe, draw 10 ml of WFI from the ampoule.
- Slowly add 10 ml WFI into the vial of OMEPRAZOLE injection and make sure the syringe is completely empty.
- Rotate and shake the vial to ensure adequate mixing of omeprazole and WFI.
- Reconstituted intravenous solution should be used immediately. After reconstitution with WFI, the stability of OMEPRAZOLE injection is 4 hours at temperature below 25°C.
Warnings and precautions:
- Before giving omeprazole to patients with gastric ulcers the possibility of malignancy should be excluded since omeprazole may mask symptoms and delay diagnosis.
- Omeprazole inhibits the metabolism of some drugs metabolized by the hepatic cytochrome P450 enzyme system and may increase plasma concentrations of diazepam, phenytoin, and warfarin.
Impaired hepatic function
Patients with impaired hepatic function show a markedly increased bioavailability, a reduced total plasma clearance and up to a fourfold prolongation of the elimination half-life. However urinary recovery over 96 hours remains unchanged, indicating no accumulation of omeprazole or its metabolites. The normal dose of omeprazole 20 mg daily may be used in patients with severe hepatic disease.
Use in pregnancy
There are no adequate or well controlled studies in pregnant women. Omeprazole should only be given to pregnant women if its use is considered essential.
Use in lactation
Although omeprazole is excreted at low concentration in the milk of lactating female rats, it is not known if omeprazole or its metabolites appear in human breast milk. Therefore it is recommended that omeprazole not be used during breastfeeding.
Omeprazole is generally well tolerated. The following adverse experiences have been reported in individuals receiving omeprazole therapy in controlled clinical situations: headache, diarrhea, abdominal pain, nausea, vomiting, upper respiratory tract infections, vertigo, rash, constipation, cough, asthenia, back pain, etc.
Most adverse reactions have been mild and transient and there has been no consistent relationship with the treatment.
Omeprazole is metabolized via the hepatic cytochrome P450 system and may be expected to interact with the pharmacokinetics of other drugs metabolized by this system. The absence of an interaction with either theophylline or propanolol suggests that omeprazole interacts with only a limited number of drugs metabolized by the cytochrome P450 system. Of the drugs studied to date, omeprazole has only demonstrated an interaction with diazepam, phenytoin, and warfarin.
Following repeated oral dosing of omeprazole 40 mg once daily the mean elimination half-life of diazepam was increased 130% with a consequent significant increase in plasma diazepam concentrations. Consideration should be given to a reduction in diazepam dosage when omeprazole is co-prescribed.
Oral omeprazole 40 mg daily for seven days reduced plasma clearance of intravenous phenytoin and increased the elimination half-life by 27%. It is recommended that the plasma concentration of phenytoin be monitored in patients co-prescribed omeprazole and phenytoin.
Concomitant administration of oral omeprazole 20 mg to healthy volunteers caused a slight though statistically significant increase in the plasma concentration of the R-enantiomer of warfarin. Plasma concentrations of the more potent S-enantiomer were not affected. A small but statistically significant increase in warfarin's anticoagulant activity accompanied this stereoselective interaction. It is recommended that coagulation tests be monitored closely when initiating or ceasing omeprazole in patients co-prescribed warfarin.
The absorption of some drugs might be altered due to the decreased intragastric acidity. Therefore it can be predicted that the absorption of ketoconazole will decrease during omeprazole treatment, as it does during treatment with other acid secretion inhibitors or antacids.
To date there has been no experience with deliberate overdosage, nor there has been any indication that omeprazole has acute toxic effects in humans. As in all cases where overdosing is suspected, treatment should be supportive and symptomatic.
Presentation and registration number:
Box, 10 vial @ 40 mg, GKL1105045544A1
ON MEDICAL PRESCRIPTION ONLY.
STORE AT TEMPERATURE BELOW 25ºC, PROTECT FROM LIGHT.
PT Ferron Par Pharmaceuticals
PT Dexa Medica