Instruction for use: Emanera

Active substance Esomeprazol

ATX code A02BC05 Esomeprazol

Pharmacological group

Proton pump inhibitors

Nosological classification (ICD-10)

K21 Gastroesophageal reflux

Biliary reflux esophagitis, gastrocardiac syndrome, Gastroesophageal reflux disease, Gastro-oesophageal reflux disease, Non-erosive reflux disease, syndrome gastrocardiac, Remhelda syndrome, Erosive reflux esophagitis, Ulcerative reflux esophagitis

K21.0 Gastro-oesophageal reflux with oesophagitis

Reflux gastritis, Reflux esophagitis, Erosive and ulcerative esophagitis

K25 Gastric ulcer

Helicobacter pylori, Pain syndrome in gastric ulcer, Pain syndrome in gastric ulcer and duodenal ulcer, Inflammation of the gastric mucosa, Inflammation of the gastrointestinal mucosa, Benign gastric ulcer, The disease of the stomach and duodenum, asotsiirovannoe with Helicobacter pylori, Aggravation gastroduodenita on the background of peptic ulcer, Exacerbation of peptic ulcer, The aggravation of gastric ulcer, The organic gastrointestinal disease, Peptic ulcer of the stomach and duodenum, Postoperative gastric ulcer, Recurrent ulcers, Symptomatic gastric ulcers, Chronic inflammatory disease of the upper gastrointestinal tract, associated with Helicobacter pylori, Helicobacter pylori eradication, Erosive and ulcerative lesions of the stomach, Erosive lesions of the stomach, The erosion of the gastric mucosa, Peptic ulcer disease, Stomach ulcer, Gastric lesion, Ulcerative lesions of the stomach, Symptomatic ulcers of the stomach and duodenum

K26 Duodenal Ulcer

Pain with duodenal ulcer, Pain syndrome in gastric ulcer and duodenal ulcer, The disease of the stomach and duodenum, asotsiirovannoe with Helicobacter pylori, Exacerbation of peptic ulcer, The worsening of duodenal ulcer, Peptic ulcer of the stomach and duodenum, Relapse of duodenal ulcers, Symptomatic ulcers of the stomach and duodenum, Helicobacter pylori eradication, Erosive and ulcerative lesions of the duodenum, Erosive-ulcerative lesions of duodenal ulcers associated with Helicobacter pylori, Erosive lesions of the duodenum, Duodenal ulcer, Ulcerative lesions of the duodenum]

K27 Peptic ulcer, unspecified

Perforation of peptic ulcer, Drug-induced gastrointestinal ulcers, medication ulcers, Peptic ulcer of the digestive tract, Peptic ulcer with Helicobacter pylori, peptic ulcer, Damage of gastrointestinal mucosa caused by NSAID, Symptomatic ulcers digestive tract, stress ulcer, Stress gastric ulcer, Stress damage to the mucous membrane, stress ulcer, duodenal ulcer Stress, Stress ulcer, Stressful GI ulcers, Erosive-ulcerative lesions of the gastrointestinal tract, The erosion of the gastrointestinal tract, Erosion of the mucosa of the upper gastrointestinal tract, The erosion of the gastrointestinal mucosa, gastrointestinal ulcer, ulcer drug, peptic ulcer, postoperative ulcer, stress ulcer, Ulcerative lesions of the gastrointestinal tract, Acute stress ulcer gastrointestinal tract, Symptomatic gastrointestinal ulcers, Complications of peptic ulcers

K31.8.2 * Hyperacidity of gastric juice

Pathological hypersecretion, Hyperacid indigestion, Hyperadic states, Increased secretion of gastric juice, Increased acid formation, Hyperacidosis,Hyper secretion of gastric juice, Increased acidity of gastric juice, High acidity

K86.8.3 * Zollinger-Ellison Syndrome

Adenoma of the pancreas ulzerogennosti, gastrinoma, Zollinger-Ellison Syndrome, gastrinoma

K92.2 Gastro-intestinal bleeding, unspecified

Gastric and intestinal bleeding, Acute bleeding from the upper gastrointestinal tract, gastrorrhagia, Gastrointestinal bleeding, Intraoperative abdominal bleeding, enterorrhagia, Bleeding in the upper digestive tract, Gastrointestinal bleeding, Bleeding from the upper gastrointestinal tract, Bleeding from the gastrointestinal tract, Intraoperative bleeding abdominal, Recurrent bleeding in the digestive tract, Diagnosis of bleeding from the small intestine, peptic ulcer bleeding, Mallory-Weiss syndrome, Recurrent bleeding from peptic ulcers, Bleeding stomach

Y45 adverse reactions in therapeutic use of analgesic, antipyretic and anti-inflammatory agents

Composition

(contains on average 14.5% of water (loss in weight on drying)

Enteric capsules 1 caps.

Pellet core:

active substance:

magnesium esomeprazole 20,645 mg

41.29 mg

(equivalent to esomeprazole — 20 or 40 mg)

excipients: sugar grits (contains sucrose and starch syrup) - 35.58 / 71.16 mg; Povidone K30 - 7.5 / 15 mg; sodium lauryl sulfate - 0.9 / 1.8 mg

pellet shell: Opadry II white 85F28751 (polyvinyl alcohol - 9.376 / 18.752 mg; titanium dioxide (E171) - 5.86 / 11.72 mg; macrogol 3000 - 4.735 / 9.47 mg; talc - 3.496 / 6.938 mg) - 23 , 44 / 46.88 mg; magnesium hydroxycarbonate (magnesium carbonate heavy) - 3/6 mg; methacrylic acid and ethyl acrylate copolymer (1: 1); dispersion 30% * - 127.49 / 254.98 mg; talc - 11.925 / 23.85 mg; macrogol 6000 - 3.825 / 7.65 mg; titanium dioxide (E171) - 3.825 / 7.65 mg; Polysorbate 80 - 1.72 / 3.44 mg

empty gelatin capsules

case: iron dye red oxide (E172) - 0.014 / 0.114 mg; titanium dioxide (E171) - 0.406 / 0.458 mg; gelatin ** - 28.38 / 45.028 mg

cap: iron dye red oxide (E172) - 0.01 / 0.076 mg; titanium dioxide (E171) - 0.271 / 0.305 mg; gelatin ** - 18.92 / 30.019 mg

* dispersion Eudragit L30D contains, in addition to methacrylic acid, copolymer ethyl acrylate and water, also sodium lauryl sulfate (0.7% based on the solid in the dispersion) and polysorbate 80 (2.3% based on the solid in the dispersion) as emulsifiers

** contains on average 14.5% of water (loss in mass during drying)

Description of the dosage form

Capsules, 20 mg: ¹ 3. Case and cap light pink color.

Capsules, 40 mg: No. 1. Case and cap from pink to pink with a slightly grayish tint.

Capsule contents: pellets from white to almost white.

pharmachologic effect

Pharmacological action - anti-ulcer.

Pharmacodynamics

Esomeprazole is the S-isomer of omeprazole and inhibits the secretion of hydrochloric acid in the stomach due to a specific and directed mechanism of action.

It specifically inhibits the proton pump of parietal cells. Both isomers of omeprazole, R- and S-, have similar pharmacodynamic activity.

Mechanism of action

Esomeprazole is a weak base, so it accumulates and becomes active in the highly acidic environment of the secretory tubules of the parietal cells of the gastric mucosa, where it inhibits the activity of the enzyme H + / K + -ATPase. Suppresses both basal and stimulated secretion of hydrochloric acid.

Effect on gastric acid secretion

The effect develops within 1 hour after ingestion of 20 mg or 40 mg of esomeprazole. With repeated intake of 20 mg of esomeprazole 1 time per day for 5 days, the average peak concentration of hydrochloric acid after stimulation with pentagastrin is reduced by 90% (on the 5th day of therapy after 6-7 hours after taking the drug).

In patients with GERD and the presence of clinical symptoms after daily intake of esomeprazole at a dose of 20 or 40 mg for 5 days, the pH of the stomach contents above 4 was maintained, on average, for 13 and 17 hours, respectively. The proportion of patients taking esomeprazole at a dose of 20 mg / day, in which the pH of the gastric contents exceeded 4 for 8, 12 and 16 hours, respectively, was 76%, 54% and 24%, and for esomeprazole 40 mg / day - 97 %, 92% and 56%.

The degree of inhibition of acid secretion by esomeprazole is directly dependent on AUC.

Therapeutic effect achieved by suppressing acid secretion

Healing of reflux esophagitis, when taking esomeprazole in a dose of 40 mg, occurs in approximately 78% of patients after 4 weeks and in 93% of patients after 8 weeks of therapy.

Treatment with esomeprazole at a dose of 20 mg 2 times a day for 1 week in combination with appropriate antibiotics leads to successful eradication of Helicobacter pylori in 90% of patients.

In case of uncomplicated peptic ulcer after eradication therapy (lasting from 7 to 10-14 days), the continuation of monotherapy with antisecretory drugs is not required to heal the ulcer and eliminate the symptoms.

Other effects associated with suppression of acid secretion

During therapy with antisecretory drugs, the level of gastrin in serum increases in response to a decrease in acid secretion.

In some patients, after prolonged therapy with esomeprazole, an increase in the number of enterochromaffin-like (ELC) cells was observed, probably due to an increase in the level of gastrin in the blood plasma.

With long-term use of antisecretory drugs, there has been a slight increase in the frequency of formation of glandular gastric cysts. These changes are due to physiological changes as a result of prolonged suppression of acid secretion. The cysts are benign and are reversible.

A decrease in the acidity of the gastric contents while receiving antisecretory agents is accompanied by an increase in the content of microbial flora in the stomach, which is present in the gastrointestinal tract in normal conditions. Therapy with proton pump inhibitors can lead to a slight increase in the risk of gastrointestinal infections, such as those caused by bacteria of the genus Salmonella and Campylobacter spp.

Esomeprazole is more effective for the healing of gastric ulcers in patients who use nonsteroidal anti-inflammatory drugs (NSAIDs), including selective COX-2 inhibitors compared with ranitidine.

High ezomeprazole effectiveness was noted in the prevention of gastric and duodenal ulcers in patients taking NSAIDs (for patients older than 60 years and / or with a peptic ulcer in history), including selective COX-2 inhibitors.

Pharmacokinetics

Suction and distribution

Esomeprazole is unstable in an acidic environment; therefore, it is ingested in the form of enteric capsules containing pellets of the preparation, the shell of which is also resistant to the action of gastric juice. In vivo, a small portion of the esomeprazole is converted to the R isomer. Esomeprazole is rapidly absorbed, reaching Cmax in the blood plasma approximately 1–2 hours after ingestion. Absolute bioavailability is 64% after administration of a single dose of 40 mg and increases to 89% with daily intake of esomeprazole 1 time per day. Bioavailability for esomeprazole at a dose of 20 mg is 50 and 68%, respectively. Vss in healthy volunteers is approximately 0.22 l / kg. Communication with plasma proteins - 97%.

Eating slows down and reduces the absorption of esomeprazole, which has no significant clinical significance.

Metabolism and excretion

Esomeprazole is completely metabolized with the participation of cytochrome P450 isoenzymes in the liver. Most of them are metabolized with the participation of the CYP2C19 polymorphic isoenzyme, which is responsible for the formation of hydroxy and demethylated metabolites. The rest of esomeprazole is metabolized by CYP3A4 isoenzyme, which is responsible for the formation of esomeprazole sulfone, the main metabolite in blood plasma.

Total plasma clearance after a single dose is approximately 17 and 9 l / h after repeated administration. T1 / 2 is 1.3 hours with long-term use of the drug 1 time per day. AUC increases with repeated use. The dose-dependent increase in AUC with repeated use is non-linear due to a decrease in metabolism during the first passage through the liver, decreased clearance, probably caused by inhibition of the CYP2C19 isoenzyme by esomeprazole and / or its sulfa-containing metabolite. With a single daily dose, esomeprazole is completely eliminated from the blood plasma during the interval between doses.

Esomeprazole does not accumulate. The major metabolites of esomeprazole do not affect the secretion of hydrochloric acid in the stomach. Almost 80% of the orally administered esomeprazole dose is excreted by the kidneys as metabolites, and the rest through the intestines. Less than 1% of unchanged esomeprazole is found in the urine.

Pharmacokinetics in certain groups of patients

In about (2.9 ± 1.5)% of the population, the activity of the CYP2C19 isoenzyme is reduced. In these patients, the metabolism of esomeprazole is carried out mainly by CYP3A4 isoenzyme. After repeated administration of esomeprazole at a dose of 40 mg 1 time per day, the average AUC value is about 2 times higher than in patients with reduced CYP2C19 activity. The average value of plasma Cmax increases by approximately 60%.

In elderly patients (71–80 years), the metabolism of esomeprazole does not change significantly.

After a single dose of 40 mg of esomeprazole, the average AUC value in women is about 30% higher than in men. Subsequently, with systematic daily intake of esomeprazole 1 time per day, differences in pharmacokinetics in patients of both sexes were not observed. These features do not affect the dose and method of use of the drug.

Esomeprazole metabolism may be impaired in people with mild or moderate hepatic impairment. The metabolic rate is reduced in severe liver dysfunction, which is accompanied by a twofold increase in AUC. Therefore, the maximum daily dose of esomeprazole in these patients is 20 mg.

The study in patients with reduced kidney function was not conducted. Since not the esomeprazole itself but its metabolites are eliminated through the kidneys, the metabolism of esomeprazole in these patients does not change.

After repeated administration of 20 and 40 mg of esomeprazole, the levels of AUC and the time to reach Cmax in children aged 12–18 years and adults were the same.

Indications of Emanera®

Gastroesophageal reflux disease (GERD):

- treatment of erosive reflux esophagitis;

- long-term maintenance treatment after healing of erosive reflux esophagitis in order to prevent relapse;

- symptomatic treatment of GERD;

stomach ulcer and duodenal ulcer;

as part of combination antibiotic therapy for the eradication of Helicobacter pylori:

- duodenal ulcer associated with Helicobacter pylori;

- prevention of recurrence of peptic ulcers associated with Helicobacter pylori;

patients taking long-term NSAIDs:

- the healing of gastric ulcers associated with taking NSAIDs;

- prevention of gastric and duodenal ulcers associated with the intake of NSAIDs in patients at risk;

long-term prevention of recurrence of repeated bleeding from peptic ulcers (after i / v use of drugs that lower the secretion of gastric glands);

Zollinger-Ellison syndrome and other conditions characterized by increased gastric secretion, including idiopathic hypersecretion.

Contraindications

hypersensitivity to esomeprazole, substituted benzimidazoles, or drug components;

simultaneous use with atazanavir and nelfinavir (see "Interaction");

hereditary intolerance to fructose;

glucose-galactose malabsorption syndrome or sucrase-isomaltase deficiency;

Children up to 12 years old (there are no data on efficacy and safety) and over 12 years old - for other indications, except gastroesophageal reflux disease (GERD).

With care: a heavy renal failure (experience of use is limited).

pregnancy and lactation

The use of the drug Emaner during pregnancy is possible only if the expected benefit to the mother exceeds the possible risk to the fetus, since insufficient data on the use of esomeprazole in pregnant women.

In epidemiological studies during the use of the racemic mixture of omeprazole, no fetotoxic effects or fetal developmental disorders were detected.

In studies with esomeprazole in animals, no direct or indirect negative effect on the development of the embryo or fetus was detected; also, no direct or indirect negative effect on the course of pregnancy, childbirth and the postnatal period of the newborn was revealed.

At present, it is not known whether esomeprazole is excreted in breast milk; therefore, Emaner should not be used during breastfeeding.

Side effects

Classification of the incidence of side effects WHO: very often ≥1 / 10; often from ≥1 / 100 to <1/10; infrequently - from ≥1 / 1000 to <1/100; rarely from ≥1 / 10000 to <1/1000; very rarely from <1/10000; frequency unknown - cannot be estimated based on available data.

In each group, unwanted effects are presented in order of decreasing severity.

On the part of the nervous system: often - headache; infrequently - insomnia, dizziness, paresthesias, drowsiness; rarely - depression, agitation, confusion; very rarely - hallucinations, aggressive behavior.

On the part of the respiratory system: rarely - bronchospasm.

On the part of the digestive system: often - abdominal pain, constipation, diarrhea, flatulence, nausea, vomiting; infrequently - dryness of the oral mucosa, increased activity of liver enzymes; rarely - stomatitis, gastrointestinal candidiasis, hepatitis (with or without jaundice); very rarely - liver failure, hepatic encephalopathy in patients with a history of liver disease.

On the part of the urinary system: very rarely - interstitial nephritis.

Reproductive system: very rarely - gynecomastia.

On the part of the musculoskeletal system: rarely - arthralgia, myalgia; very rarely - muscle weakness.

For the skin: infrequently - dermatitis, skin rash, pruritus, urticaria; rarely - alopecia, photosensitivity; very rarely - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the side of blood-forming organs: rarely - leukopenia, thrombocytopenia; very rarely - agranulocytosis, pancytopenia.

On the part of the senses: infrequently - blurred vision; rarely - a change in taste.

Allergic reactions: rarely hypersensitivity reactions (for example, fever, angioedema, anaphylactic reaction / anaphylactic shock).

Laboratory data: rarely - hyponatremia; very rarely - hypomagnesemia, hypocalcemia due to severe hypomagnesemia, hypokalemia due to severe hypomagnesemia.

Other: infrequent - peripheral edema; rarely - sweating; very rarely - weakness (malaise).

Interaction

Effect of esomeprazole on the pharmacokinetics of other drugs

Drugs, the absorption of which depends on the pH level. Reducing the secretion of hydrochloric acid in the stomach during treatment with esomeprazole and other proton pump inhibitors may lead to changes in the absorption of drugs, the absorption of which depends on the acidity of the medium. Like antacids and other drugs that reduce gastric acidity, esomeprazole may reduce the absorption of ketoconazole, itraconazole and erlotinib, and increase the absorption of drugs such as digoxin.

The simultaneous use of omeprazole in a dose of 20 mg 1 time per day and digoxin increases the bioavailability of digoxin by 10% (the bioavailability of digoxin increased by up to 30% in 2 out of 10 patients).

It is known about the interaction of omeprazole with some antiretroviral drugs. The mechanism and clinical significance of these interactions are not always known. Reducing the acidity of gastric juice during therapy with omeprazole may affect the absorption of antiretroviral drugs. Interaction at the level of an isoenzyme CYP2C19 is also possible. During therapy with omeprazole, a decrease in the serum concentration of some antiretroviral drugs (atazanavir and nelfinavir) has been observed. Therefore, simultaneous use is not recommended. The simultaneous use of omeprazole (40 mg once a day) with atazanavir 300 mg / ritonavir 100 mg in healthy volunteers is accompanied by a marked decrease in the exposure to atazanavir (AUC, Cmax and Cmin in plasma decreased by about 75%). Increasing the dose of atazanavir to 400 mg did not compensate for the effects of omeprazole on the bioavailability of atazanavir.

With simultaneous use of omeprazole with saquinavir, serum concentration of saquinavir increases.

Given the similar pharmacokinetic and pharmacodynamic properties of omeprazole and esomeprazole, the simultaneous use of esomeprazole with antiretroviral drugs such as atazanavir and nelfinavir is not recommended.

CYP2C19 metabolized drugs. Esomeprazole inhibits CYP2C19, the main isoenzyme of the metabolism of esomeprazole. Thus, with simultaneous use of esomeprazole with drugs whose metabolism involves the CYP2C19 isoenzyme, such as diazepam, citalopram, imipramine, clomipramine, phenytoin, etc., the concentration of these drugs in the blood plasma may increase and, accordingly, their dose reduction may be required .

This is especially necessary to take into account when prescribing the drug Emanera® as needed. Thus, with simultaneous use with 30 mg of esomeprazole, clearance of diazepam (substrate of CYP2C19 isoenzyme) is reduced by 45%.

The simultaneous use of esomeprazole in a dose of 40 mg leads to an increase in the concentration of phenytoin in the blood plasma of patients with epilepsy by 13%.

It is recommended to control the concentration of phenytoin in the blood plasma at the beginning of therapy with esomeprazole and with its abolition.

With the use of omeprazole at a dose of 40 mg, the Cmax and AUC of voriconazole (substrate of CYP2C19 isoenzyme) are increased by 15 and 41%, respectively.

The coagulation time with simultaneous long-term administration of warfarin and esomeprazole at a dose of 40 mg remains within acceptable limits. However, several cases of a clinically significant increase in the INR index have been reported. It is recommended to control INR at the beginning and at the end of the simultaneous use of esomeprazole and warfarin or other coumarin derivatives.

The use of omeprazole at a dose of 40 mg led to an increase in Cmax and AUC of Cilostazol by 18 and 26%, respectively; for one of the active metabolites of Cilostazol, the increase was 29 and 69%, respectively.

The simultaneous use of esomeprazole in a dose of 40 mg with cisapride leads to an increase in the values of pharmacokinetic parameters of cisapride in healthy volunteers: AUC - by 32% and T1 / 2 - by 31%, however, Cmax does not significantly change. The slight lengthening of the QT interval on the ECG, which is observed with cisapride monotherapy, did not increase with the addition of esomeprazole.

In some patients, an increase in serum methotrexate concentration was noted against the background of simultaneous use with proton pump inhibitors. When using high doses of methotrexate, the possibility of temporary withdrawal of esomeprazole should be considered.

Esomeprazole does not cause clinically significant changes in the pharmacokinetics of amoxicillin and quinidine.

Simultaneous short-term use of esomeprazole and naproxen or rofecoxib showed no clinically significant pharmacokinetic interaction.

In a clinical study, the interaction with the use of clopidogrel (300 mg — loading dose, then 75 mg / day) with omeprazole (80 mg) simultaneously, at the same time for 5 days was studied. The activity of the thiol metabolite (active metabolite) of clopidogrel was reduced by 46% (1st day of therapy) and 42% (5th day of therapy), while taking clopidogrel and omeprazole at the same time. When clopidogrel and omeprazole were taken at the same time, the mean suppression of platelet aggregation (IPA) was reduced by 47% (during 24 hours of therapy) and 30% (5th day of therapy).

According to the results of another study: omeprazole, when used with clopidogrel, not simultaneously, at different times, has no inhibitory effect on the CYP2C19 isoenzyme. In the studies, conflicting data on the clinical manifestations of clopidogrel interaction with major cardiovascular events were recorded.

With simultaneous use with tacrolimus, an increase in serum tacrolimus concentrations is possible.

The effect of drugs on the pharmacokinetics of esomeprazole

CYP2C19 and CYP3A4 isoenzymes are involved in the metabolism of esomeprazole. With simultaneous use of esomeprazole with clarithromycin (500 mg 2 times a day) (inhibitor of the isoenzyme CYP3A4), the AUC value of esomeprazole increases by 2 times.

The simultaneous use of esomeprazole and the combined inhibitor of CYP2C19 and CYP3A4 isoenzymes, for example, voriconazole, may be accompanied by an increase in the AUC of esomeprazole by more than 2 times. Usually, in such situations, no change in the dose of esomeprazole is required. In patients with severely impaired liver function or, if necessary, long-term therapy, the question of reducing the dose of esomeprazole should be resolved.

Drugs that induce CYP2C19 and CYP3A4 isoenzymes, such as rifampicin and Hypericum perforatum drugs, when used simultaneously with esomeprazole, can lead to a decrease in the concentration of esomeprazole in the blood plasma due to the acceleration of the metabolism of esomeprazole.

Dosage and administration

Inside, without chewing, washing down with a small amount of liquid.

For patients with difficulty swallowing, pour the contents of the capsules into half a glass of non-carbonated water, stir and drink immediately or within 30 minutes. Then re-fill the glass with water by half, rinse the walls of the glass and drink.

Do not mix the drug with other liquids, because This may lead to the dissolution of the pellet containment shell. Pellets should not be chewed or crushed.

Patients who cannot swallow on their own should dissolve the contents of the capsules in non-carbonated water and inject esomeprazole through a nasogastric tube. It is necessary to check the compliance of the syringe for the injection and the probe. Instructions on the preparation and administration of the drug through a nasogastric tube are given in the subsection "Dosing the drug through a nasogastric tube".

Adults and teenagers over 12 years old

GERD:

- Erosive reflux esophagitis (treatment): 40 mg 1 time per day for 4 weeks. If after the first course of therapy, the healing of esophagitis does not occur or symptoms persist, an additional 4-week course of treatment with esomeprazole is recommended.

- Long-term maintenance treatment after healing of erosive reflux esophagitis to prevent relapse: 20 mg 1 time per day.

- Symptomatic treatment of GERD: 20 mg 1 time per day - for patients without esophagitis. If after 4 weeks of treatment it was not possible to achieve control of the symptoms, it is necessary to re-examine the patient. After the symptoms are eliminated, you can continue taking the drug Emaner on demand, i.e. take 20 mg of the drug 1 time per day if symptoms occur. Patients taking NSAIDs that are at risk of developing gastric or duodenal ulcers are not recommended treatment on demand.

Adult patients

Peptic ulcer and duodenal ulcer

As part of combination antibacterial therapy for the eradication of Helicobacter pylori:

- Duodenal ulcer associated with Helicobacter pylori and prevention of recurrence of peptic ulcer associated with Helicobacter pylori (Helicobacter pylori combined eradication therapy includes: Emanera 20 mg, amoxicillin 1 g and clarithromycin 500 mg). All drugs are taken 2 times a day, 7-14 days.

Patients for a long time taking NSAIDs:

- Healing of stomach ulcers associated with taking NSAIDs: 20 mg or 40 mg 1 time per day for 4–8 weeks.

- Prevention of gastric and duodenal ulcers associated with taking NSAIDs in patients at risk: Emanera 20 mg or 40 mg once a day.

Long-term prevention of recurrence of recurrent bleeding from peptic ulcers (after intravenous administration of drugs that lower the secretion of gastric glands): Emanera 40 mg once a day for 4 weeks after the onset of recurrent bleeding.

Zollinger-Ellison syndrome and other conditions characterized by increased gastric secretion, including idiopathic hypersecretion: the initial dose of the drug Emaner 40 mg 2 times a day. The dose of the drug and the duration of treatment are selected individually depending on the clinical picture of the disease. The disease in most patients is controlled by taking the drug in a dose of 80 to 160 mg / day. If necessary, the use of the drug Emaner more than 80 mg / day, the daily dose is divided into two doses.

Impaired renal function. Patients with impaired renal function dose change is not required. Experience with the use of esomeprazole in patients with severe renal insufficiency is limited; In this regard, in the appointment of the drug in such patients should be careful.

Liver dysfunction. Patients with mild or moderate hepatic impairment are not required to change the dose. In severe liver failure, the maximum daily dose should not exceed 20 mg.

Elderly patients. Elderly patients dose adjustment is not required.

Nasogastric tube administration

When prescribing the drug through a nasogastric tube, it is necessary:

1. Open the capsule and pour the contents of the capsule into a special syringe. Add 25 ml of drinking water and about 5 ml of air to the syringe. Some probes may require dilution of the product in 50 ml of drinking water in order to prevent the pellets contained in the capsule from clogging the probe.

2. After adding water, immediately shake the syringe until a suspension is obtained.

3. Make sure that the tip is not clogged (slightly pressing down on the piston, keeping the syringe in position with the tip up).

4. Insert the syringe tip into the probe, continuing to hold it upwards.

5. Shake the syringe and tip it upside down. Immediately inject 5–10 ml of the dissolved drug into the probe. After the introduction of the solution, return the syringe to its previous position and shake (the syringe should be kept tip up to avoid clogging the tip).

6. Again, lower the syringe tip down and inject another 5–10 ml of solution into the probe. Repeat the procedure until the syringe is empty.

7. In case of residual part of the preparation in the form of sediment in the syringe: fill the syringe with 25 ml of water and 5 ml of air and repeat the procedures described in paragraphs 5 and 6. For some probes, 50 ml of drinking water may be needed for this purpose.

Overdose

To date, cases of overdose of the drug Emaner not described. Ingestion of esomeprazole at a dose of 280 mg was accompanied by general weakness and symptoms of the gastrointestinal tract. A single intake of 80 mg of esomeprazole was not accompanied by any symptoms. A specific antidote does not exist. Esomeprazole is actively associated with plasma proteins, so hemodialysis is ineffective.

Treatment: in case of overdose, symptomatic therapy should be carried out.

special instructions

If anxious symptoms appear (such as significant spontaneous weight loss, repeated vomiting, dysphagia, vomiting with blood or melena), as well as suspected or detected gastric ulcers, it is necessary to exclude a malignant neoplasm, since the use of Emanera can reduce the severity of symptoms and delay making a diagnosis.

Patients who have been taking Emaner for a long time (especially for more than a year) should be under regular medical supervision.

Patients taking the drug on demand should be informed of the need to consult a doctor when symptoms change.

Given the fluctuations in the concentration of esomeprazole in the blood plasma when using the drug in the on-demand mode, interactions with other drugs should be considered (see "Interaction").

When using esomeprazole for the eradication of Helicobacter pylori, possible interactions between the components of triple therapy should be considered. Clarithromycin is a potent inhibitor of CYP3A4; therefore, contraindications and drug interactions of clarithromycin should be considered when prescribing triple therapy to patients who are simultaneously taking drugs metabolized by CYP3A4, such as cisapride.

The drug Emaner contains sucrose, therefore, its use is contraindicated in patients with hereditary fructose intolerance, glucose-galactose malabsorption syndrome or sucrase-isomaltase deficiency.

Impact on the ability to drive vehicles and other complex mechanisms. The drug Emanera does not affect the control of vehicles and work with other technical devices, requiring increased concentration of attention and speed of psychomotor reactions.

Release form

Enteric capsules, 20 mg, 40 mg. 7 caps. in the blister of the combined material oriented polyamide / aluminum / PE + desiccant and aluminum foil + PE or of the combined material oriented polyamide / aluminum / PVC and aluminum foil. On 1, 2, 4 blisters are placed in a cardboard box.

Pharmacy sales terms

On prescription.

Storage conditions

At temperatures not higher than 25 ° C, in the original packaging.

Keep out of the reach of children.

Shelf life

2 years.

Do not use after the expiration date printed on the package.