Index of drugs

aDULTi. Gastroesophageal reflux disease: treatment of erosive reflux oesophagitis; long-term use in patients with cured oesophagitis to prevent relapse; symptomatic treatment of gastroesophageal reflux disease. Combination therapy with appropriate antibacterial drugs for eradicationHelicobacter pylori,treatment of duodenal ulcer associated with infectionH. pylori,prevention of recurrent peptic ulcers in patients with peptic ulcer associated with infectionH. pylori. For patients who require continuous treatment with NSAIDs: treatment of stomach ulcers associated with NSAID treatment; prevention of gastric and duodenal ulcer associated with NSAID treatment in at-risk patients. Long-term treatment after intravenous prevention of recurrent bleeding from peptic ulcers. Treatment of Zollinger-Ellison syndrome.Adolescents aged> 12 years. Gastroesophageal reflux disease: treatment of erosive reflux oesophagitis; long-term use in patients with cured oesophagitis to prevent relapse; symptomatic treatment of gastroesophageal reflux disease. In combination with antibiotics, treatment of duodenal ulcer caused byHelicobacter pylori.

1 tabl enteral contains 20 mg or 40 mg of esomeprazole (and 16.13 mg and 32.26 mg of sugar seeds respectively, sugar granules consisting of sucrose and maize starch, sucrose content of approx. 80-91.5%, Glucose ≤5%).

Esomeprazole (S-isomer of omeprazole) is 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. Both Omeprazole isomers (R and S) have similar pharmacodynamic effects. Esomeprazole is unstable in an acidic environment, which is why it is administered orally in the form of coated enteric granules. In conditionsin vivo conversion to the R isomer does not play a significant role. Absorption of esomeprazole is rapid and C_max occurs about 1-2 hours after administration. The absolute bioavailability is 64% after a single 40 mg dose and increases to 89% after repeated once-daily dosing. The corresponding values ​​after a 20 mg dose are 50% and 68%. It is 97% bound to plasma proteins. Esomeprazole is completely metabolised by cytochrome P450. The main role in the metabolism of esomeprazole is played by the polymorphic isoenzyme CYP2C19, responsible for the formation of the hydroxy and demethyl metabolites of 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. Almost 80% of the oral dose of esomeprazole is excreted in the form of metabolites in the urine and the remainder in the faeces. Less than 1% of the parent drug is detected in the urine. 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.

Hypersensitivity to the active substance, benzimidazole derivatives or any of the excipients. Do not use with nelfinavir.

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. Patients who have been on treatment for a long time (especially if the treatment lasts for more than a year) should remain under regular medical supervision. Treatment with esomeprazole may result in a slight increase in the risk of gastrointestinal infections with such bacteria asSalmonella spp. And Campylobacter spp.and in hospitalized patients as wellClostridium difficile. Esomeprazole may reduce the absorption of vitamin B₁₂ (cyanocobalamin) due to hypo or achlorhydria; this should be taken into account during long-term treatment of patients with reduced vitamin B stores₁₂ or risk factors for its reduced absorption. 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. Es Omeprazole, 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). If esomeprazole is prescribed for eradicationHelicobacter pylori, possible interactions of all components of triple therapy (including Clarithromycin, a strong CYP3A4 inhibitor) should be considered. The use of esomeprazole in children aged <12 years is not recommended. Due to the glucose and sucrose content, the drug should not be used in patients with rare hereditary disorders associated with fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase deficiency.

Data from epidemiological studies on a larger number of pregnant women do not show that omeprazole (racemic mixture) causes developmental or fetotoxic effects. Caution should be exercised when prescribing to pregnant women. It is not known whether esomeprazole is excreted in human milk, therefore the medicine should not be used during breast-feeding.

Common: headache, abdominal pain, constipation, diarrhea, bloating, nausea and / or vomiting. Uncommon: peripheral edema, insomnia, central dizziness, paresthesia, drowsiness, labyrinthine dizziness, dry mouth, increased liver enzymes, dermatitis, pruritus, rash, urticaria, hip fracture, wrist or spine. Rare: leukopenia, thrombocytopenia, hypersensitivity reactions (eg fever, angioneurotic edema and anaphylactic reaction or shock), hyponatremia, psychomotor agitation, confusion, depression, taste disturbances, blurred vision, bronchospasm, oral mucositis, gastrointestinal tidiness, hepatitis with jaundice or without jaundice, alopecia, hypersensitivity to light, joint pain, muscle pain, unwellness, increased sweating. Very rare: agranulocytosis, pancytopenia, aggressiveness, 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 not known: hypomagnesaemia (severe hypomagnesaemia may correlate with hypocalcaemia), microscopic colitis.

Orally.Adults and adolescents aged> 12 years. Gastroesophageal reflux disease: treatment of erosive reflux oesophagitis - 40 mg once daily for 4 weeks (in patients whose esophagitis has not been cured or whose symptoms persist, treatment is recommended to continue for the Next 4 weeks); long-term use in patients with cured oesophagitis to prevent relapse - 20 mg once a day; symptomatic treatment of gastroesophageal reflux disease - 20 mg once a day in patients without oesophagitis (if the symptoms have not been controlled after 4 weeks, further tests should be performed, after symptoms disappear further control of the symptoms can be obtained by administering 20 mg once a day; in adults, the drug can be administered as an adjunct in a dose of 20 mg once a day, if necessary, in patients treated with NSAIDs at risk of gastric ulcer and duodenal ulcer, ad hoc administration is not recommended in case of recurrence of ailments).Adults. Combination therapy with appropriate antibacterial drugs for eradicationhelicobacter pylori (also the treatment of duodenal ulcer associated with infectionH. pylori and prevention of recurrent peptic ulcers in patients with peptic ulcer associated with infectionH. pylori): 20 mg esomeprazole and 1 g Amoxicillin and 500 mg of Clarithromycin (all medicines should be given twice daily for 7 days).For patients who require continuous NSAID treatment: treatment of stomach ulcers associated with NSAID treatment - 20 mg once a day for 4-8 weeks; prevention of gastric and duodenal ulcer associated with NSAID treatment in at-risk patients - 20 mg once a day.Long-term treatment after intravenous prevention of recurrent bleeding from peptic ulcers: 40 mg once daily for 4 weeks after intravenous treatment to prevent recurrent bleeding from peptic ulcers.Treatment of Zollinger-Ellison syndrome: the recommended starting dose is 40 mg 2 times a day; this dose should then be adjusted to the individual patient's needs and continued for as long as there are clinical indications; available clinical data indicate that the majority of patients can be controlled with doses in the range of 80-160 mg esomeprazole per day; doses> 80 mg / day should be given in divided doses (twice a day).Adolescents aged> 12 years. Treatment of duodenal ulcer caused byH. pylori. The choice of the appropriate combination therapy should take into account the official national, regional and local guidelines regarding bacterial resistance, duration of treatment (usually 7 days, but sometimes up to 14 days) and the proper use of antibacterial drugs. The course of treatment should be supervised by a specialist. 30-40 kg body weight: 20 mg esomeprazole and 750 mg amoxicillin and 7.5 mg / kg body weight clarithromycin (all medicines should be given twice a day for a week); mc. > 40 kg: 20 mg esomeprazole and 1 g amoxicillin and 500 mg of clarithromycin (all medicines should be given twice a day for a week).Special groups of patients. In the elderly, in patients with impaired renal function and in patients with mild to moderate hepatic impairment no dose adjustment is required. In patients with severe hepatic impairment, a dose of> 20 mg / day should not be used. In patients with severe renal impairment, care should be taken. Use in children <12 years is not recommended.Way of giving. The tablets should be swallowed whole without chewing or chewing, with liquid. For patients who have difficulty swallowing, the tablets can also be mixed with 1/2 glass of still water. No other liquids should be used as the enteric coating may dissolve. The tablet with water should be stirred until the tablet disintegrates. The liquid with pellets should be drunk immediately or within 15 minutes. Then fill the glass halfway with water, stir and drink. Pellets should not be chewed or chewed. For patients who can not swallow, the tablets can be mixed with still water and administered through the stomach tube.