Esopraz® Powder for injection, each vial contains : Esomeprazole sodium equivalent to Esomeprazole 40 mg.
Esopraz® with Esomeprazole sodium (equivalent to Esomeprazole) as active ingredient is available in 40 mg powder for injection.
Esomeprazole injection is indicated for :
Gastric antisecretory treatment when the oral route is not possible, such as :
- Gastroesophageal reflux disease (GERD) in patients with esophagitis and/or severe symptoms of reflux.
- Healing of gastric ulcers associated with NSAID therapy.
The short term maintenance of hemostasis and prevention of rebleeding in patients following therapeutic endoscopy for acute bleeding gastric or duodenal ulcers.
DOSAGE AND ADMINISTRATIONS :
Gastric antisecretory treatment when the oral route is not possible :
- Patients who cannot take oral medication may be treated parenterally with 20 – 40 mg once daily. Patients with reflux esophagitis should be treated with 40 mg once daily. Patients treated symptomatically for reflux disease should be treated with 20 mg once daily.
- For healing of gastric ulcers associated with NSAID therapy the usual dose is 20 mg once daily. For prevention of gastric and duodenal ulcers associated with NSAID therapy, patients at risk should be treated with 20 mg once daily.
- Usually the intravenous treatment duration is short and transfer to oral treatment should be made as soon as possible.
Prevention of rebleeding of gastric and duodenal ulcers :
- Following therapeutic endoscopy for acute bleeding gastric or duodenal ulcers, 80 mg should be administered as a bolus infusion over 30 minutes, followed by a continuous intravenous infusion of 8 mg/hour given over 3 days (72 hours).
- The parenteral treatment period should be followed by oral acid-suppression therapy.
Children and adolescents
Esomeprazole IV should not be used in children and adolescents since no data is available.
Impairment renal function
Dose adjustment is not required in patients with impaired renal function. Due to limited experience in patients with severe renal insufficiency, such patients should be treated with caution.
Impairment hepatic function
GERD : Dose adjustment is not required in patients with mild to moderate liver impairment. For patients with severe liver impairment, a maximum daily dose of 20 mg Esomeprazole IV should not be exceeded.
Bleeding ulcers : Dose adjustment is not required in patients with mild to moderate liver impairment. For patients with severe liver impairment, following an initial bolus dose of 80 mg Esomeprazole for infusion, a continuous intravenous infusion dose of 4 mg/hour may be sufficient.
Dose adjustment is not required in the elderly.
- FOR SINGLE USE ONLY, any unused solution should be discarded.
- The reconstituted solution should be inspected usually for particulate matter and discoloration prior to administration. Only clear solution should be used.
A solution for injection is prepared by adding 5 ml of 0.9 % Sodium chloride for intravenous use in Esomeprazole 40 mg vial.
40 mg dose
5 ml of the reconstituted solution should be given as an intravenous injection over a period of at least 3 minutes.
20 mg dose
2.5 ml or half of the reconstituted solution should be given as an intravenous injection over a period of at least 3 minutes. Any unused solution should be discarded.
10 mg dose
1.25 ml of the reconstituted solution should be given as an intravenous injection over a period of at least 3 minutes. Any unused solution should be discarded.
A solution for infusion is prepared by dissolving the content of one vial with Esomeprazole 40 mg in up to 100 ml of 0.9 % Sodium chloride for intravenous use.
40 mg dose
The reconstituted solution should be given as an intravenous infusion over a period of 10 – 30 minutes.
20 mg dose
Half of the reconstituted solution should be given as an intravenous infusion over a period of 10 – 30 minutes. Any unused solution should be discarded.
10 mg dose
A quarter of the reconstituted solution should be given as an intravenous infusion over a period of 10 – 30 minutes. Any unused solution should be discarded.
80 mg bolus dose
A solution for infusion is prepared by dissolving the contents of two vials of Esomeprazole 40 mg in up to 100 ml of 0.9 % Sodium chloride for intravenous use.
The reconstituted solution should be given as a continuous intravenous infusion over 30 minutes.
8 mg/hour dose
The reconstituted solution should be given as a continuous intravenous infusion over a period of 71.5 hours (calculated rate of infusion of 8 mg/hour).
- The reconstituted solution for injection and infusion is clear and colourless to very slightly yellow.
- The degradation of reconstituted solution is highly pH dependent and the product must therefore only be reconstituted in the specified volume of 0.9 % Sodium chloride for intravenous use. The reconstituted solution should not be mixed or co-administered in the same infusion set with any other drug. The reconstituted solution should be administered separately from other drugs.
- Esomeprazole should not be used continuously with drugs such as Atazanavir and Nelvinavir.
- Hypersensitivity to the active substance Esomeprazole or to other substituted Benzimidazoles or to any of the excipients of this medicinal product.
WARNINGS AND PRECAUTIONS :
- 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, malignancy should be excluded, as treatment with Esomeprazole may alleviate symptoms and delay diagnosis.
- Treatment with proton pump inhibitors may lead to slightly increased risk of gastrointestinal infections such as Salmonella and Campylobacter.
- Co-administration of Esomeprazole with Atazanavir is not recommended. If the combination of Atazanavir with a proton pump inhibitors is judged unavoidable, dose clinical monitoring is recommended in combination with an increase in the dose of Atazanavir to 400 mg with 100 mg of Ritonavir; Esomeprazole 20 mg should not be exceeded.
- Esomeprazole is a CYP2C19 inhibitor. When starting or ending treatment with Esomeprazole, the potential for interaction with drug metabolized through CYP2C19 should be considered. An interaction is observed between Clopidogrel and Omeprazole. The clinical relevance of this interaction is uncertain. As a precaution, concomitant use of Esomeprazole and Clopidogrel should be discouraged.
- Esomeprazole should be used during pregnancy only if clearly needed.
- Because Esomeprazole is likely to be excreted in human milk, women should discontinued breast-feeding.
DRUG INTERACTIONS :
- The absorption of Ketoconazole and Itraconazole can decrease during treatment with Esomeprazole.
- When Esomeprazole is combined with drugs metabolized by CYP2C19, such as Diazepam, Citalopram, Imipramine, Clomipramine, Phenytoin etc., the plasma concentrations of these drugs may be increased and a dose reduction could be needed. It is recommended to monitor the plasma concentrations of Phenytoin when treament with Esomeprazole is introduced or withdrawn.
- Monitoring is recommended when initiating and ending concomitant Esomeprazole treatment during treatment with warfarin or other coumarine derivatives.
- Esomeprazole has been shown to have no clinically relevant effects on the pharmacokinetics of Amoxicillin or Quinidine.
- Concomitant administration of Esomeprazole and a combined inhibitor of CYP2C19 and CYP3A4, such as Voriconazole, may result in more than doubling of the Esomeprazole exposure.
ADVERSE REACTIONS :
Blood and lymphatic system disorders
Rare : Leukopenia, thrombocytopenia.
Very rare : Agranulocytosis, pancytopenia.
lmmune system disorders
Rare : Hypersensitivity reactions e.g., fever, angioedema and anaphylactic reaction/shock.
Metabolism and nutrition disorders
Uncommon : Peripheral edema.
Rare : Hyponatraemia.
Not known : Hypomagnesaemia.
Uncommon : Insomnia.
Rare : Agitation, confusion, depression.
Very rare : Aggression, hallucinations.
Nervous system disorders
Common : Headache.
Uncommon : Dizziness, paraesthesia, somnolence.
Rare : Taste disturbance.
Uncommon : Blurred vision.
Ear and labyrinth disorders
Uncommon : Vertigo.
Respiratory, thoracic and mediastinal disorders
Rare : Bronchospasm.
Common : Abdominal pain, constipation, diarrhoea, flatulence, nausea/vomiting.
Uncommon : Dry mouth.
Rare : Stomatitis, gastrointestinal candidiasis.
Uncommon : Increased liver enzymes.
Rare : Hepatitis with or without jaundice.
Very rare : Hepatic failure, encephalophaty in patients with pre-existing liver disease.
Skin and subcutaneous tissue disorders
Common : Administration site reactions.
Uncommon : Dermatitis, pruritus, rash, urticaria.
Rare : Alopecia, photosensitivity.
Very rare : Erythema multiforme, Stevens-johnson syndrome, toxic epidermal necrolysis (TEN).
Musculoskeletal, connective tissue and bone disorders
Rare : Arthralgia, myalgia.
Very rare : Muscular weakness.
Renal and urinary disorders
Very rare : Interstitial nephritis.
Reproductive system and breast disorders
Very rare : Gynaecomastia.
General disorders and administration site conditions
Rare : Malaise, increased sweating.
Esopraz® Powder for injection 40 mg Box, 1 vial @ 40 mg
Reg. No. : DKL2002360944A1
STORE BELOW 30ºC, PROTECT FROM LIGHT
Reconstituted solution is stable in storage for 12 hours at a temperature below 30°C.
ON MEDICAL PRESCRIPTION ONLY
Manufactured by :
Sidoarjo – Indonesia