Inhibition of gastric acidity when oral esomeprazole is not possible: gastroesophageal reflux disease in patients with oesophagitis and / or severe reflux symptoms; treatment of stomach ulcers associated with NSAID treatment; prevention of gastric and duodenal ulcers associated with NSAID treatment in patients at risk. Prevention of bleeding recurrence after endoscopic treatment due to acute bleeding from gastric or duodenal ulcer.
Composition:
One vial contains 40 mg esomeprazole (as a sodium salt).
Action:
S-isomer of Omeprazole, a specific proton pump inhibitor (H+/ K+ ATPase) in the parietal cells of the gastric mucosa. It reduces the secretion of hydrochloric acid in the stomach, both basal and stimulated. The drug is 97% bound to plasma proteins. It is completely metabolised by cytochrome P450. The main role in the metabolism is played by the polymorphic isoenzyme CYP2C19, responsible for the formation of hydroxyl and demethyl metabolites esomeprazole. The rest of the drug is metabolised by the CYP3A4 isoenzyme, which is responsible for the formation of esomeprazole sulfone - the main metabolite found in the blood. The esomeprazole AUC increases after repeated administration of the drug. This phenomenon depends on the dose of the drug and is nonlinear. This is due to reduced first-pass effect and reduced systemic clearance, probably due to inhibition of CYP2C19 enzyme by esomeprazole and / or its sulfonated metabolite. T0,5 in the blood in the elimination phase, after repeated once daily administration, is about 1.3 hours. The drug is excreted in the form of metabolites in the urine (80%), partly in the faeces; <1% of the dose is excreted in urine unchanged. In slow metabolisers (who do not have active CYP2C19 isoenzyme), mean maximum blood concentrations were greater by about 60% than in fast metabolisers (those with active CYP2C19 isoenzyme) - these observations do not affect the dosage of esomeprazole. In patients with hepatic impairment the metabolic rate is reduced.
Contraindications:
Hypersensitivity to the active substance, other benzimidazole derivatives or any of the excipients. Co-administration with nelfinavir.
Precautions:
In patients with suspected or diagnosed peptic ulcer disease, as well as any disturbing symptoms (eg significant unintentional weight loss, recurrent vomiting, difficulty swallowing, bloody vomiting or tarry stools), the cancerous background of the disease should be excluded, as esomeprazole treatment may alleviate the symptoms of cancer and delay its diagnosis. Treatment with esomeprazole may result in a slight increase in the risk of gastrointestinal infections with such bacteria asSalmonella spp. And Campylobacter spp. Patients treated with esomeprazole for at least 3 months (in most cases for a year) have experienced severe hypomagnesaemia; in patients who are envisaged for long-term treatment or who are taking proton pump inhibitors concomitantly with Digoxin or hypomagnesaemic agents (eg diuretics), Magnesium determination should be considered prior to initiating esomeprazole treatment and then periodically during treatment. Proton pump inhibitors can increase the overall risk of fractures by 10-40%; Patients at risk of osteoporosis should receive care in accordance with current clinical guidelines, and provide adequate amounts of vitamin D and calcium. Use with caution in patients with severe renal impairment. Esomeprazole, as a CYP2C19 inhibitor, may interact with drugs that are metabolised by this isoenzyme - be careful. Co-administration of esomeprazole and Clopidogrel should be avoided. The use of esomperazole with atazanavir is not recommended (reduction of atazanavir exposure).
Pregnancy and lactation:
Limited data are available on the use of esomeprazole during pregnancy. Animal studies do not indicate direct or indirect harmful effects of esomeprazole on embryo or fetal development.Studies on racemic mixtures made on animals do not indicate direct or indirect harmful effects on pregnancy, parturition or postnatal development. Caution should be used when using esomeprazole during pregnancy. It is not known whether esomeprazole is excreted in human milk, therefore the medicine should not be used during breast-feeding.
Side effects:
Common: headache, abdominal pain, constipation, diarrhea, bloating, nausea, vomiting, injection site reactions (if high doses are used for 3 days). Uncommon: peripheral edema, insomnia, dizziness, paresthesia, drowsiness, blurred vision, labyrinthine dizziness, dry mouth, increased liver enzymes, dermatitis, pruritus, rash, urticaria, hip fracture, carpal bones or spine. Rare: leukopenia, thrombocytopenia, hypersensitivity reactions (ie fever, angioneurotic edema and anaphylactic reaction, shock), hyponatremia, agitation, confusion, depression, taste disorders, bronchospasm, stomatitis, fungal infection (candidiasis) of the gastrointestinal tract, hepatitis (with jaundice or without jaundice), hair loss, hypersensitivity to light, joint pain, muscle pain, feeling unwell, alopecia, hypersensitivity to light, joint pain, muscle pain, feeling unwell, increased sweating. Very rare: agranulocytosis, pancytopenia, aggression, hallucinations, hepatic failure, encephalopathy in patients with pre-existing liver disease, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, muscle weakness, interstitial nephritis, gynecomastia. Frequency unknown: hypomagnesemia. In isolated cases, in critically ill patients who received Omeprazole (racemate) by intravenous injections, especially at high doses, there were irreversible visual disturbances; no cause and effect relationship has been established with drug administration.
Dosage:
Intravenously.Inhibition of gastric secretion when oral administration is not possible: reflux oesophagitis - 40 mg once a day; symptomatic gastro-oesophageal reflux - 20 mg once a day; treatment of stomach ulcers associated with the use of NSAIDs - usually 20 mg once a day; prevention of gastric and duodenal ulcers associated with NSAID treatment in patients at risk - 20 mg once a day. Intravenous therapy is usually short and oral treatment should be started as soon as possible.Prevention of bleeding recurrence after endoscopic treatment due to acute bleeding from gastric or duodenal ulcer: 80 mg infusion over 30 min, followed by continuous infusion for 3 days (72 h) at a dose of 8 mg / h. After intravenous therapy, treatment with acid secretion should be continued orally for 4 weeks.Special groups of patients. No dosage adjustment is necessary in the elderly, in patients with renal insufficiency or mild to moderate hepatic impairment. Caution should be exercised in patients with severe renal impairment. In patients with severe hepatic impairment: in gastroesophageal reflux disease, a daily dose of 20 mg should not be exceeded; in ulcer bleeding, after administration of 80 mg in a short-term infusion, intravenous infusion may be sufficient for 71.5 hours at a dose of 4 mg / h. It should not be used in children and adolescents due to a lack of data on safety and efficacy.Way of giving. It can be given by injection into a vein lasting at least 3 minutes (20 mg and 40 mg) or as an infusion lasting 10-30 minutes (dose 20 mg and 40 mg) or 30 min (dose 80 mg); giving 20 mg by injection or infusion, give half of the prepared solution, giving 40 mg or 80 mg of all the prepared solution. The dose of 8 mg / h should be given as a continuous infusion lasting 71.5 h; the infusion rate should be 8 mg / h.
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