Index of drugs

Adults. Gastroesophageal reflux disease: treatment of erosive reflux oesophagitis, long-term use to prevent the recurrence of reflux oesophagitis, symptomatic treatment of gastroesophageal reflux disease. In combination with appropriate antibiotic treatment regimens to eradicate the infectionHelicobacter pylorias well as in the treatment of duodenal ulcer with the infectionHelicobacter pylori and in the prevention of recurrent gastric and duodenal ulcer in patients with ulceration coexisting with infectionHelicobacter pylori. Patients requiring treatment with non-steroidal anti-inflammatory drugs (NSAIDs): treatment of stomach ulcers caused by NSAID treatment, prevention of gastric and duodenal ulcers associated with the use of NSAIDs in at-risk patients. Long-term treatment after intravenous therapy used preventively against recurrent bleeding from peptic ulcers. Zollinger-Ellison syndrome.Youth from the age of 12. Gastroesophageal reflux disease: treatment of erosive reflux oesophagitis, long-term use to prevent the recurrence of reflux oesophagitis, symptomatic treatment of gastroesophageal reflux disease. In combination with antibiotics for the treatment of duodenal ulcer caused by infectionHelicobacter pylori.

1 enteral capsules contain 20 mg or 40 mg of esomeprazole (in the form of Magnesium esomeprazole dihydrate). The drug contains sucrose and p-hydroxybenzoates.

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. 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. Accordingly, after the 20 mg dose, the above values ​​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 esomeprazole, benzimidazole derivatives or to any of the excipients. Do not use in combination 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. 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. 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). 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 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. The drug contains p-hydroxybenzoates, which can cause an allergic (also delayed) reaction.

Data from epidemiological studies on 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, dizziness, paresthesia, drowsiness, labyrinthine dizziness, dry mouth, increased liver enzymes, dermatitis, pruritus, rash, urticaria, fracture of the hip, wrist or spine. Rare: leukopenia, thrombocytopenia, hypersensitivity reactions (eg fever, angioneurotic edema and anaphylactic reaction or shock), hyponatraemia, psychomotor agitation, confusion, depression, taste disturbances, blurred vision, bronchospasm, oral mucositis, gastrointestinal candidiasis, hepatitis with jaundice or without jaundice, alopecia, hypersensitivity to light, joint pain, muscle pain, unwellness, increased sweating. Very rare: agranulocytosis, pancytopenia, aggressiveness, hallucinations, hepatic insufficiency, encephalopathy in patients with pre-existing liver disease, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, muscle weakness, interstitial nephritis (some patients have been reported at the same time renal failure), 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 to prevent relapse - 20 mg once a day; symptomatic treatment of gastroesophageal reflux disease - 20 mg once daily in patients without oesophagitis (if after 4 weeksthe symptoms have not been controlled, further tests should be performed, after the symptoms have resolved, further control of the symptoms can be obtained by administering the drug at a dose of 20 mg once a day; in adults, the medicine 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 the 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.Way of giving. The capsules should be swallowed whole and washed with liquid; they should not be chewed or crushed. If you have difficulty swallowing, the capsule can be opened and dissolved in half a glass of still water. Do not dissolve the contents of the capsules in any other liquid, because the coating to protect the contents from the effects of gastric juice can be damaged. The solution with visible granules should be mixed and drunk immediately or within 30 minutes of preparation. Then fill the glass half with water, stir and drink. Do not chew or crush granules. If the patient can not swallow by himself, the contents of the capsule can be dissolved in still water and administered by gavage into the stomach.