Inhibition of gastric secretion when oral administration is not possible: gastroesophageal reflux disease in patients with oesophagitis and / or severe reflux symptoms; treatment of stomach ulcers associated with the treatment of non-steroidal anti-inflammatory drugs; prevention of gastric and duodenal ulcers associated with the treatment of non-steroidal anti-inflammatory drugs 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. It is 97% bound to plasma proteins. It is metabolised in the liver, mainly by cytochrome P450 CYP2C19 isozyme (for hydroxylated and demethylated derivatives) and partly by the CYP3A4 isoenzyme (for sulphonic derivative). In patients with normal CYP2C19 isoenzyme (so-called rapid metabolic) T0,5 after repeated once-daily administration it is about 1.3 hours. The drug is excreted mainly in the form of metabolites - 80% of the dose in the urine, the remainder in the faeces. In patients with mild to moderate hepatic insufficiency, esomeprazole metabolism may be slowed. In patients with severe hepatic impairment, total exposure to esomeprazole is 2-fold increased. In patients with impaired renal function no changes in the metabolism of esomeprazole should be expected.
Contraindications:
Hypersensitivity to esomeprazole, other benzimidazole derivatives or other components of the preparation. Co-administration with nelfinavir. Children.
Precautions:
The use of the preparation with atazanavir is not recommended. Use with caution in patients with severe renal impairment.
Pregnancy and lactation:
Due to limited data from studies, the drug should be used with caution in pregnancy. Do not use during breast-feeding.
Side effects:
Common: headache, abdominal pain, constipation, diarrhea, bloating, nausea or vomiting, reactions at the injection site. Uncommon: peripheral edema, insomnia, dizziness, paresthesia, drowsiness, blurred vision, labyrinthine dizziness, dry mouth, increased liver enzymes, dermatitis, pruritus, rash, urticaria. Rare: leukopenia, thrombocytopenia, hypersensitivity reactions (fever, angioneurotic edema and anaphylactic reaction, shock), hyponatraemia, agitation, confusion, depression, taste disorders, bronchospasm, stomatitis, fungal infection (candidosis) of the gastrointestinal tract, hepatitis with jaundice or without, hair loss, hypersensitivity to light, muscle or joint pain, unwellness, 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. In isolated cases, in critically ill patients who received Omeprazole (racemate) by intravenous injections, especially at high doses, there were irreversible visual disturbances. A cause and effect relationship has not been established with drug administration. Treatment with proton pump inhibitors may slightly increase the risk of infection of the gastrointestinal tract with bacteria of the genusSalmonella andCamphylobacter.
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. Gastric ulcer caused by NSAID treatment: 20 mg once a day. Patients at risk (for the prevention of stomach and duodenal ulcers): 20 mg once a day. You should go to oral therapy 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 to suppress acid secretion should be continued. It can be given by injection into a vein lasting at least 3 minutes or as an intravenous infusion lasting 10-30 minutes (dose 20 mg and 40 mg) or 30 minutes (dose 80 mg). The dose of 8 mg / h should be given as a continuous infusion lasting 71.5 h; the infusion rate should not exceed 8 mg / h. No dosage adjustment is necessary in the elderly, in patients with renal insufficiency or mild to moderate hepatic impairment. In patients with severe hepatic impairment, a daily dose of 20 mg should not be exceeded. In patients with severe hepatic insufficiency, in the prevention of ulcer bleeding, after administration of 80 mg in a short-term infusion, an intravenous infusion for 71.5 hours at a dose of 4 mg / h may be sufficient.