EZOMIN [Esomeprazole] 20 mg Capsules

instructions for the medical use of a medicinal product

EZOMIN

Tradename

Ezomin, Эзомин

International non-proprietary name or generic name

Эзомепразол, Esomeprazole

Dosage form

Capsules.

Composition

Each enteric-coated capsule contains: Esomeprazole magnesium trihydrate equiv. esomeprazole USP 40 mg

Pharmacotherapeutic group

Antiulcer agents.

Code АТХ: A02BC05

Pharmacological properties

Pharmacodynamics

An inhibitor of H+-K+-ATPase, a dextrorotatory isomer of omeprazole. Reduces the secretion of hydrochloric acid in the stomach by specifically inhibiting the proton pump in parietal cells. Being a weak base and passing into an active form in the acidic environment of the secretory canals of the parietal cells of the gastric mucosa, it activates and inhibits the proton pump - the enzyme H+-K+-ATPase. Inhibits both basal and stimulated secretion of hydrochloric acid. The effect occurs 1 hour after oral administration of 20 mg or 40 mg. With daily use for 5 days at a dose of 20 mg once a day, the average maximum concentration of hydrochloric acid after stimulation with pentagastrin is reduced by 90%.

Pharmacokinetics

After oral administration, esomeprazole is rapidly absorbed. Cmax in blood plasma is achieved after 1-2 hours. The absolute bioavailability of esomeprazole after a single dose of 40 mg is 64% and increases to 89% with daily administration once a day. For a dose of 20 mg esomeprazole, these figures are 50% and 68%, respectively. Plasma protein binding is 97%. Esomeprazole is metabolized by the cytochrome P450 system. The main part is metabolized with the participation of a specific polymorphic isoenzyme CYP2C19, with the formation of hydroxylated and demethylated metabolites of esomeprazole. The metabolism of the remainder is carried out by the isoenzyme CYP3A4; with the formation of a sulfo derivative of esomeprazole, which is the main metabolite determined in plasma. The total clearance is approximately 17 l/h after a single dose of esomeprazole and 9 l/h after multiple doses. T1/2 is 1.3 h with systematic administration in a once-daily dosing regimen. AUC increases with repeated administration (nonlinear dependence of dose and AUC with systematic administration, which is a consequence of a decrease in metabolism during the first pass through the liver, as well as a decrease in systemic clearance caused by inhibition of the CYP2C19 enzyme by esomeprazole and/or its sulfo-containing metabolite). Does not accumulate. Up to 80% of the dose is excreted in the form of metabolites by the kidneys (less than 1% - unchanged), the rest is excreted with bile.

Indications for use

- gastroesophageal reflux disease (GERD: treatment of erosive reflux esophagitis; long-term maintenance treatment after healing of erosive reflux esophagitis to prevent relapse; symptomatic treatment of GERD);

- gastric ulcer and duodenal ulcer;

- as part of combination antibacterial therapy (for Helicobacter pylori eradication: duodenal ulcer associated with Helicobacter pylori; prevention of relapse of peptic ulcer associated with Helicobacter pylori);

- patients taking long-term nonsteroidal anti-inflammatory drugs (NSAIDs): healing of gastric ulcer associated with NSAIDs; prevention of gastric ulcer associated with NSAIDs in patients at risk;

- long-term prevention of recurrent bleeding from peptic ulcers (after intravenous administration of drugs that reduce the secretion of gastric glands); - Zollinger-Ellison syndrome and other conditions characterized by increased gastric secretion, including idiopathic hypersecretion.

Contraindications

- hypersensitivity to esomepromazole;

- children under 12 years of age and children over 12 years of age for other indications, except for gastroesophageal reflux disease;

- concomitant use of esomeprazole with atazanavir and nelfinavir.

Method of administration and dosage

Orally, without chewing, with a small amount of liquid.

Adults and children over 12 years of age

Gastroesophageal reflux disease (GERD):

- erosive reflux esophagitis (treatment): 40 mg once a day for 4 weeks. If after the first course of therapy the esophagitis does not heal or symptoms persist, an additional 4-week course of treatment is recommended;

- long-term maintenance treatment after healing of erosive reflux esophagitis to prevent relapse: 20 mg once a day;

- symptomatic treatment of GERD: 20 mg once a day - in patients without esophagitis. If after 4 weeks of therapy it was not possible to achieve control of symptoms, it is necessary to re-examine the patient. After the symptoms have disappeared, you can continue taking the drug as needed, i.e. take 20 mg of the drug once a day when symptoms occur.

Patients taking NSAIDs who are at risk of developing gastric or duodenal ulcers are not recommended to receive treatment on an as-needed basis.

Adults

Gastric and duodenal ulcers

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

Helicobacter pylori-associated duodenal ulcers and prevention of relapses of Helicobacter pylori-associated peptic ulcers: the combination eradication therapy for Helicobacter pylori includes: Ezomin—20 mg, amoxicillin—1 g, and clarithromycin—500 mg. All drugs are taken 2 times a day for 7–14 days.

Patients taking NSAIDs for a long time:

- healing of gastric ulcer associated with NSAIDs: 20 or 40 mg once a day for 4-8 weeks.

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

Long-term prevention of recurrent bleeding from peptic ulcers (after intravenous use of drugs that reduce the secretion of gastric glands): 40 mg once a day for 4 weeks after the start of intravenous prevention of recurrent bleeding.

Zollinger-Ellison syndrome and other conditions characterized by increased gastric secretion, including idiopathic hypersecretion: the initial dose of the drug is 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. In most patients, the disease is controlled by taking the drug at a dose of 80 to 160 mg per day. If it is necessary to use the drug in excess of 80 mg per day, the daily dose is divided into two doses.

Special instructions and precautions

Consult a physician before using the drug.

In the presence of symptoms such as significant spontaneous weight loss, frequent vomiting, dysphagia, vomiting with blood or melena, as well as in the presence (or suspicion) of a gastric ulcer, the possibility of a malignant neoplasm should be excluded, since treatment with esomeprazole may lead to smoothing of symptoms and, thus, delay the correct diagnosis.

During long-term therapy, the patient's condition should be regularly monitored.

During treatment with proton pump inhibitors, the plasma gastrin level increases as a result of reduced intragastric secretion of hydrochloric acid. In patients taking proton pump inhibitors for a long time, the formation of glandular cysts in the stomach is more common. These phenomena are due to physiological changes as a result of inhibition of hydrochloric acid secretion. Esomeprazole, like all acid-reducing drugs, may result in decreased absorption of vitamin B12 due to hypo- or achlorhydria. This should be considered in patients with risk factors for decreased absorption of vitamin B12 during long-term therapy.

When using proton pump inhibitors, especially when used in high doses and over a long period (> 1 year), the risk of fractures of the femoral neck, carpal bones and vertebrae increases (especially in elderly patients).

Esomeprazole can cause an increase in the level of chromogranin A, which can distort the results of examinations for neuroendocrine tumors. Treatment should be temporarily suspended at least 5 days before determining chromogranin A.

Influence on the ability to drive vehicles and machinery

During the period of drug use, patients should be careful when driving vehicles and machinery, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Application during pregnancy and during breastfeeding

Use during pregnancy is possible in cases where the expected benefit of therapy for the mother exceeds the possible risk to the fetus. Contraindicated for use during breastfeeding.

Side effect

From the digestive system: abdominal pain, constipation, diarrhea, flatulence, nausea/vomiting, dry mouth.

From the nervous system: headache, dizziness, paresthesia, drowsiness, taste disturbance.

From the skin and subcutaneous tissues: dermatitis, itching, rash, urticaria, alopecia, photosensitivity, injection site reactions, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

From the musculoskeletal system: arthralgia, myalgia, muscle weakness.

Mental disorders: insomnia, depression, agitation, hallucinations.

From the liver and biliary tract: increased activity of liver enzymes, hepatitis (with and without jaundice).

From the hematopoietic system: leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.

From the respiratory system: bronchospasm.

From the organ of vision: blurred vision.

Allergic reactions: hypersensitivity reactions (eg, fever, angioedema, anaphylactic reaction/anaphylactic shock).

Others: peripheral edema, malaise, sweating.

If any of the side effects listed in the instructions worsen, or you notice any other side effects not listed in the instructions, tell your doctor.

Interaction with other medicinal products

It is believed that with simultaneous use, it is possible to increase plasma concentrations and enhance the effects of imipramine, clomipramine, citalopram.

With simultaneous use, it is possible to decrease plasma concentrations and clinical efficacy of itraconazole and ketoconazole.

It is possible with simultaneous use to increase plasma concentrations of diazepam and phenytoin, which, apparently, is of no clinical significance.

A decrease in the secretion of hydrochloric acid in the stomach during treatment with esomeprazole and other proton pump inhibitors can lead to a decrease or increase in the absorption of drugs whose absorption depends on the acidity of the environment.

With the simultaneous use of esomeprazole and tacrolimus, an increase in the concentration of tacrolimus in the blood plasma was noted.

In some patients, an increase in the concentration of methotrexate was noted during concomitant use with proton pump inhibitors. When using high doses of methotrexate, the possibility of temporary withdrawal of esomeprazole should be considered. There are data that the combined use of esomeprazole with clarithromycin, which inhibits the CYP3A4 isoenzyme, leads to a 2-fold increase in the AUC of esomeprazole. Concomitant use of esomeprazole and a combined inhibitor of CYP3A4 and CYP2C19 isoenzymes, such as voriconazole, may lead to a more than 2-fold increase in the AUC of esomeprazole.

Medicines that induce CYP2C19 and CYP3A4 isoenzymes, such as rifampicin and St. John's wort, when co-administered with esomeprazole, may lead to a decrease in the concentration of esomeprazole in the blood plasma due to the acceleration of its metabolism.

Overdose

Symptoms: general weakness and gastrointestinal symptoms.

Treatment: symptomatic therapy. Specific antidote unknown. Poorly eliminated by dialysis.

Storage conditions

Store in a dry, dark place at a temperature not exceeding 25 °C.

Keep out of reach of children.

Shelf life

3 years. Do not use after the expiration date stated on the package.

Vacation conditions

Dispensed by prescription.

Release form

14 capsules in an aluminum foil blister. 2 blisters together with instructions for use in a cardboard box.