Esozid

Esomeprazole sodium

Each vial contains: Esomeprazole sodium equivalent to Esomeprazole 40 mg.

Pharmacology: Pharmacodynamics: Esomeprazole a proton pump inhibitor, is the S-isomer of omeprazole.
Esomeprazole is a weak base and is concentrated and converted to the active form in the highly acidic environment of the secretory canaliculi of the parietal cell.
It specifically inhibits the enzyme H⁺/K⁺-ATPase in the acid pump and inhibits both basal and stimulated acid secretion. Esomeprazole blocks the final step in acid production, resulting in potent, long-lasting inhibition of gastric and secretion.
Pharmacokinetics: Distribution: The apparent volume of distribution as steady state in healthy subject is approximately 16 L. Esomeprazole is 97% plasma protein bound.
Metabolism and excretion: Esomeprazole is completely metabolized by the cytochrome P450 (CYP) isoenzyme CYP2C19 and the remainder is metabolized by the cytochrome P450 (CYP) isoenzyme CYP3A4. The major metabolites of esomeprazole have no effect on gastric acid secretion. The plasma elimination half-life is about 1.3 hours.
Esomeprazole is completely eliminated from plasma between doses with no tendency for accumulation during once daily administration.

ESOZID IV for injection and infusion is indicated for: Gastric anti-secretory treatment when the oral route is not possible, such as: Gastro esophageal reflux disease in patients with esophagitis and/or severe symptoms of reflux; Healing of gastric ulcers associated with NSAIDs therapy.
The short term maintenance of hemostasis and prevention of rebleeding in patients following therapeutic endoscopy for acute bleeding gastric or duodenal ulcers.

Gastric anti-secretory treatment when the oral route is not possible: Patients who cannot take oral medicines may be treated parenterally with 20-40 mg once daily. Patients with reflux esophagitis should be treated with 40 mg once daily. Patients with 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. Usually the IV treatment durations short and transfer to oral treatment should be made as soon as possible.
Maintenance of hemostasis and prevention of rebleeding of gastric and duodenal ulcers following therapeutic endoscopy for acute bleeding gastric or duodenal ulcers, 80 mg should be administrated as a bolus infusion over 30 minutes, followed by continuous intravenous infusion of 8 mg/hour given over 3 days (72 hours).
The parenteral treatments period should be followed by acid-suppression therapy with esomeprazole 40 mg gastro-resistant tablet once daily for 4 weeks.
Children and adolescent: Esomeprazole IV should not be used in children and adolescent since no data is available.
Impaired hepatic function: Treatment for bleeding ulcer 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 for 71.5 hours may be sufficient.
Method of administration: Injection: 40 mg dose: The reconstituted solution should be given as an intravenous injection over a period of at last 3 minutes.
20 mg dose: Half of the reconstituted solution should be given as an intravenous injection over a period of approximately 3 minutes. Any unused solution should be discarded.
Infusion: 40 mg dose: The reconstituted solution should be given as an intravenous infusion over a period of 10 to 30 minutes.
20 mg dose: Half of the reconstituted solution should be given as an intravenous infusion over a period of 10 to 30 minutes. Any unused solution should be discarded.
80 mg bolus dose: 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).

Esomeprazole is extensively plasma protein bound and is therefore not readily dialyzable. As in any case of overdose, treatment should be symptomatic and general support measures should be utilized.

Esomeprazole should not be used continuously with drugs such as atazanavir and nelfinavir.
Hypersensitivity to the active substance esomeprazole or to other substituted benzimidazoles or to any of the excipients of this medicinal product.

In the presence of any alarming symptoms (e.g. significant unintentional weight loss, recurrent vomiting, dysphagia, hematemesis 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 inhibitor is judged unavoidable, close 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 interactions with drugs metabolized through CYP2C19 should be considered. An interaction is observed between clopidogrel and omeprazole. The clinical relevance of this interactions is uncertain. As a precaution, concomitant use of esomeprazole and clopidogrel should be discouraged.
Use in Pregnancy: Esomeprazole should be used during pregnancy only if clearly needed.
Use in Lactation: Because esomeprazole is likely to be excreted in human milk, women should discontinued breast-feeding.

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.

Blood and lymphatic system disorders: Rare: leukopenia, thrombocytopenia; Very rare: agranulocytosis, pancytopenia.
Immune system disorders: Rare: hypersensitivity reactions e,g, fever, angioedema and anaphylactic reaction/shock.
Metabolism and nutrition disorders: Uncommon: peripheral edema; Rare: hyponatraemia; Very rare: hypomagnesaemia.
Psychiatric disorders: Uncommon: insomnia; Rare: agitation, confusion, depression; Very rare: aggression, hallucinations.
Nervous system disorders: Common: headache; Uncommon: dizziness, paraesthesia, somnolence; Rare: taste disturbance.
Eye disorders: Uncommon: blurred vision.
Ear and labyrinth disorders: Uncommon: vertigo.
Respiratory, thoracic and mediastinal disorders: Rare: bronchospasm.
Gastrointestinal disorders: Common: abdominal pain, constipation, diarrhea, flatulence, nausea/vomiting; Uncommon: dry mouth; Rare: stomatitis, gastrointestinal candidiasis.
Hepatobiliary disorders: Uncommon: increased liver enzymes; Rare: hepatitis with or without jaundice; Very rare: hepatic failure, encephalopathy 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 multiform, 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.

The absorption of ketoconazole and itraconazole can decrease during treatment with esomeprazole.
Concomitant administration with esomeprazole and atazanavir is not recommended.
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 concentration of phenytoin when treatment 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 esomeprazole exposure.

Instructions for Use and Handling: Injection: A solution for injection is prepared adding 5 mL of 0.9% sodium chloride for intravenous use to the vial with esomeprazole. The reconstituted solution should be inspected visually for particulate matter and discoloration prior to administration. Only clear solution should be used.
Infusion: A solution for infusion is prepared by dissolving the content of one vial with esomeprazole in up to 100 mL of 0.9% sodium chloride for intravenous use.
Infusion 80 mg: A solution for infusion is prepared by dissolving the content of two vials with esomeprazole 40 mg in up to 100 mL of 0.9% sodium chloride for intravenous use. The reconstituted solution should be inspected visually for particulate matter and discoloration prior to administration. Only clear solution should be used.
Incompatibilities: The degradation of reconstituted solution is highly pH dependent and the product must therefore only be reconstituted in the specific volume of 0.9% sodium chloride for intravenous use. The reconstituted solution should not be mixed or co-administration in the same infusion set with any other drug.

Store at temperature below 30°C. Protect from light.
Store in the outer carton. Keep out of the reach of children.
Storage After Reconstitution: After reconstituted with 5 mL of 0.9% sodium chloride, 100 mL of 0.9% sodium chloride, and 100 mL of Ringer's lactate, ESOZID IV is stable for 12 hours if stored at temperatures below 25°C.
After reconstituted with 100 mL of 5% Dextrose, ESOZID IV is stable for 6 hours if stored at temperatures below 25°C.

Antacids, Antireflux Agents & Antiulcerants

A02BC05 - esomeprazole ; Belongs to the class of proton pump inhibitors. Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).

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