Zefxon

Zefxon

omeprazole

Manufacturer:

Biolab

Distributor:

Cathay Drug
Full Prescribing Info
Contents
Omeprazole.
Description
Each pack contains one vial and one ampoule: Each vial contains: Omeprazole sodium 42.6 mg equivalent to Omeprazole 40 mg.
Each ampoule of solvent for reconstitution contains: Propyleneglycol 4 g, Monobasic sodium phosphate, monohydrate 0.01 g, Citric acid monohydrate to adjust pH and water for injection q.s. to 10 ml.
Action
Pharmacology: Pharmacodynamics: Omeprazole (Zefxon) injection is the proton acid pump inhibitor which reduces gastric acid secretion by specific action; inhibition of the enzyme H+, K+-ATPase (The proton pump) in the parietal cell, the final step of acid secretion; thus inhibition of acid secretion occurs.
Pharmacokinetics: Distribution: The apparent volume of distribution in healthy subjects is approximately 0.3 L/kg and a similar value is also seen in patients with renal insufficiency. In the elderly and in patients with hepatic insufficiency, the volume of distribution is slightly decreased. The plasma protein binding of omeprazole is about 95%.
Metabolism and excretion: The average half-life of the terminal phase of the plasma concentration-time curve following IV administration of omeprazole is approximately 40 minutes; the total plasma clearance is 0.3 to 0.6 L/min. There is no change in half-life during treatment.
Omeprazole is completely metabolised by the cytochrome P450 system, mainly in the liver.
No metabolite has been found to have any effect on gastric acid secretion. Almost 80% of an intravenously given dose is excreted as metabolites in the urine, and the remainder is found in the faeces, primarily originating from biliary secretion.
Elimination of omeprazole is unchanged in patients with reduced renal function. The elimination half-life is increased in patients with impaired liver function, but omeprazole has not shown any accumulation with once daily oral dosing.
Indications/Uses
Omeprazole (Zefxon) injection is indicated for alternative use to oral medication in Duodenal ulcer; Gastric ulcer; Reflux oesophagitis; Zollinger-Ellison syndrome; Aspiration prophylaxis.
Dosage/Direction for Use
Omeprazole (Zefxon) injection administration once daily is recommended where oral medication is inappropriate. This produces a mean decrease over 24 hours of approximately 90%. In patients with Zollinger-Ellison syndrome the recommended initial dosage of Zefxon injection is 60 mg once daily. Higher daily doses may be required and the dose should be divided and given twice daily. For aspiration prophylaxis, Zefxon injection should be administered 1 hour before operation.
Directions for Reconstitution: For IV Injection: Dissolve Zefxon injection 1 vial with the solvent provided to get omeprazole concentration of 4 mg/mL. The IV solution should be used within 4 hours after reconstitution. Do not use if any particles are present in the reconstituted solution.
For IV infusion: Dissolve Zefxon injection 1 vial with the solvent provided to get omeprazole concentration of 4 mg/mL. Then dilute with normal saline for infusion (0.9% w/v sodium chloride) 90 mL or 5% dextrose for infusion (5% w/v of dextrose) 90 mL to make a solution of 100 mL of omeprazole with a concentration of 0.4 mg/mL. The duration of IV infusion should be 20-30 minutes. The IV solution should be used within 5 hours after reconstitution. Do not store in refrigerator and do not use if any particles are present in the reconstituted solution.
Use in children: Safety and efficacy of omeprazole in children has not been established.
Use in elderly: Normal adult dosage is recommended.
Dosage in Renal Impairment: Although pharmacokinetics may be altered in patients with renal impairment, dosage adjustment does not appear necessarily in patients with such impairment.
Dosage in Hepatic Impairment: Dosage adjustment should be considered in patients with hepatic impairment. Some clinicians recommend that such patients with hepatic impairment receiving dosage exceeding 20 mg daily should be monitored closely for possible adverse effects.
Overdosage
In the event of overdosage, treatment should be symptomatic supportive.
Contraindications
Known hypersensitivity to any component of the formulation.
Special Precautions
When gastric ulcer is suspected, the possibility of malignancy should be excluded as treatment may alleviate symptoms and delay diagnosis.
Use In Pregnancy & Lactation
Omeprazole (Zefxon) injection should not be given during pregnancy and lactation unless its use is considered essential.
Adverse Reactions
Proton pump inhibitors, by decreasing gastric acidity, may increase the risk of gastro-intestinal infections.
Omeprazole (Zefxon) injection is generally well tolerated. The following events have been reported: Central and peripheral nervous system: Headache, dizziness, paraesthesia, light headedness, feeling faint, somnolence, insomnia, vertigo, reversible mental confusion, agitation, aggression, depression, hallucinations (predominantly in severely ill patients).
Endocrine: Gynaecomastia.
Gastrointestinal: Diarrhea, constipation, abdominal pain, nausea, vomiting, flatulence, dry mouth, stomatitis, gastrointestinal candidiasis.
Hematological: leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.
Hepatic: Increased liver enzymes, encephalopathy in patients with pre-existing severe liver disease; hepatitis with or without jaundice, hepatic failure increased liver enzymes.
Musculoskeletal: Arthralgia, myalgia, muscular weakness.
Reproductive system and breast disorders: Impotence.
Skin: Rash and/or pruritus, urticaria, photosensitivity, bullous eruption, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (TEN), alopecia.
Other: Malaise, Hypersensitivity reactions e.g. angioedema, fever, bronchospasm, interstitial nephritis and anaphylactic shock. Increased sweating, peripheral edema, blurred vision, taste disturbance, hyponatraemia.
Drug Interactions
Omeprazole (Zefxon) injection may interact with other drugs metabolized by mixed function oxidase. Reduced dose of these drugs: Diazepam, Warfarin and Phenytoin has been associated with concomitant use of omeprazole.
The absorption of ketoconazole or itraconazole can decrease during omeprazole treatment due to decreased intragastric acidity.
Plasma concentrations of omeprazole and clarithromycin are increased during concomitant administration.
There may be interactions with other drugs also metabolized via the cytochrome P450 enzyme system.
Increases and decreases in serum cyclosporine concentrations have been reported with concomitant administration of cyclosporine and omeprazole. The mechanism is unknown. Until more data are available, monitoring of cyclosporine levels is recommended during concomitant therapy.
The combination of disulfiram and omeprazole may cause confusion or disorientation in some patients.
Storage
Store at temperatures not exceeding 25°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).
Presentation/Packing
Powd for inj (vial) 40 mg x 1's.
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