EZOMIN [Esomeprazole] 40 mg Powder for IV solution

EZOMIN

instructions for the medical use of the medicinal product

Tradename

Ezomin, Эзомин

International non-proprietary name or generic name

Esomeprazole, Эзомепразол

Composition

Each bottle contains:

Esomeprazole (as esomeprazole sodium) 40 mg

Dosage form

Powder for preparation of solution for injection.

Pharmacotherapeutic group

Proton pump inhibitors.

Pharmacological properties

Pharmacodynamics

Antiulcer drug - proton pump inhibitor, 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 tubules of parietal cells of the gastric mucosa, it activates and inhibits the proton pump - the enzyme H + -K + -ATP-ase. Inhibits both basal and stimulated secretion of hydrochloric (hydrochloric) acid. The effect occurs within 1 hour after oral administration of 20 mg or 40 mg. With daily use for 5 days at a dose of 20 mg 1 time per day, the average maximum concentration of hydrochloric acid after stimulation with pentagastrin decreases by 90%.

Pharmacokinetics

Antiulcer drug - proton pump inhibitor, 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 tubules of parietal cells of the gastric mucosa, it activates and inhibits the proton pump - the enzyme H + -K + -ATP-ase. Inhibits both basal and stimulated secretion of hydrochloric (hydrochloric) acid. The effect occurs within 1 hour after oral administration of 20 mg or 40 mg. With daily use for 5 days at a dose of 20 mg 1 time per day, the average maximum concentration of hydrochloric acid after stimulation with pentagastrin decreases by 90%.

Indications for use

Prodrug. Absorption - 50-64%, increases with repeated administration to approximately 68 and 89% for doses of 20 and 40 mg, respectively. The half-life is 0.5-1 hours. The connection with plasma proteins is 97%. Biotransformation in the liver is predominantly CYP2C19, to a lesser extent CYP34 with the formation of inactive metabolites. With repeated administration, there is a decrease in the effect of primary passage through the liver, probably associated with the suppression of CYP2C19 activity. Acceptance of equimolar doses of the S- and R-isomers results in a higher plasma concentration of the S- rather than the R-isomer. Creatinine clearance - 500-600 ml / min. Elimination by the kidneys 70-80% (inactive metabolite), with feces 20-30% (inactive metabolite).

Contraindications

• hypersensitivity to esomeprazole, substituted benzimidazoles;

• children under 1 year of age or body weight less than 10 kg;

• children's age 1-4 years for other indications, except for the treatment of erosive esophagitis and symptomatic treatment of GERD;

• children's age 4-11 years for other indications, except for the treatment of erosive esophagitis and symptomatic treatment of GERD and the treatment of duodenal ulcer associated with H. pylori, as part of combination therapy;

• age 12 years and older for other indications, except for GERD and treatment of duodenal ulcer associated with H. pylori, as part of combination therapy;

• combined use with atazanavir and nelfinavir.

Method of administration and dosage

Adults

As an alternative to oral therapy, if it is impossible to carry it out, intravenous administration of Esomin at a dose of 20-40 mg 1 time / day can be recommended.

For GERD in patients with esophagitis, a dose of 40 mg 1 time / day is recommended.

To treat the symptoms of GERD, Ezomin is used at a dose of 20 mg 1 time / day.

For the healing of peptic ulcers associated with taking NSAIDs in patients at risk, a dose of 20 mg 1 time / day is recommended.

For the prevention of peptic ulcers associated with taking NSAIDs, Ezomin is recommended at a dose of 20 mg 1 time / day.

As a rule, the period of treatment with the intravenous form is short, the patient should be switched to oral administration of the drug as soon as possible.

In order to prevent recurrence of bleeding from a peptic ulcer after endoscopic hemostasis, Ezomin is recommended at a dose of 80 mg as an intravenous infusion for 30 minutes, followed by an extended intravenous infusion of the drug at a dose of 8 mg / h for 3 days (72 hours). After the end of parenteral therapy, antisecretory therapy is recommended to suppress acid secretion (for example, 40 mg 1 time / day for 4 weeks).

Duration of IV injections and infusions

Injections

Dose 40 mg: prepared solution of Esomin (5 ml, 8 mg / ml) is injected intravenously for at least 3 minutes.

Dose 20 mg: half of the prepared solution of the drug (2.5 ml, 8 mg / ml) is injected intravenously for at least 3 minutes. Unused residues of the solution should be disposed of.

Infusion

Dose 40 mg: the prepared solution of Esomin is administered as an intravenous infusion for 10-30 minutes.

Dose 20 mg: half of the prepared solution of the drug is administered as an intravenous infusion for 10-30 minutes. Unused residues of the solution should be disposed of.

Dose 80 mg: prepared solution of Esomin is administered as an intravenous infusion over 30 minutes.

Dose 8 mg / h: the prepared solution of the drug is administered as an extended intravenous infusion for 71.5 hours (8 mg / h).

Children (ages 1 to 18)

As an alternative to oral therapy, if it is impossible to carry out it for GERD in patients with erosive reflux esophagitis and / or severe symptoms of reflux disease, Esomin is administered parenterally 1 time / day as part of the course of GERD therapy (dosage recommendations are presented in the table).

Ezomin dosage recommendations for children and adolescents

Duration of IV injections and infusions

Injections

Dose 40 mg: the prepared Esomin solution (5 ml, 8 mg / ml) is injected intravenously for at least 3 minutes.

Dose 20 mg: half of the prepared solution of the drug (2.5 ml, 8 mg / ml) is injected intravenously for at least 3 minutes. Unused residues of the solution should be disposed of.

Dose of 10 mg: 1.25 ml of the prepared solution of Esomin (8 mg / ml) is injected intravenously for at least 3 minutes. Unused residues of the solution should be disposed of.

Infusion

Dose 40 mg: the prepared solution of Esomin is administered as an intravenous infusion for 10-30 minutes.

Dose 20 mg: half of the prepared solution of the drug is administered as an intravenous infusion for 10-30 minutes. Unused residues of the solution should be disposed of.

Dose 10 mg: a quarter of the prepared Esomin solution is administered as an intravenous infusion over 10-30 minutes. Unused residues of the solution should be disposed of.

The period of treatment with the intravenous form should be short, the patient should be transferred to oral administration of the drug as soon as possible.

Preparation of the solution

Degradation of the prepared solution mainly depends on the pH value, and therefore only 0.9% sodium chloride solution for intravenous administration should be used to dissolve the drug.

The prepared solution should not be mixed or administered together with other drugs.

Before use, the solution should be assessed visually for the absence of visible mechanical impurities and color changes. Only a clear solution can be used. The prepared solution is recommended to be introduced immediately after preparation (from a microbiological point of view).

Solution for intravenous injection (8 mg / ml) prepared by adding 5 ml of 0.9% sodium chloride solution for intravenous administration in a vial with 40 mg of Esomin.

Solution for intravenous infusion 40 mg prepared by dissolving the contents of one vial with 40 mg of the drug in 100 ml of 0.9% sodium chloride solution for intravenous administration.

Solution for intravenous infusion 80 mg prepared by dissolving the contents of 2 vials with Ezomin 40 mg in 100 ml of 0.9% sodium chloride solution for intravenous administration.

Special instructions and precautions

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

With prolonged therapy, the patient's condition should be regularly monitored.

During treatment with proton pump inhibitors, plasma gastrin levels increase as a result of decreased intragastric secretion of hydrochloric acid. Patients taking proton pump inhibitors for a long time are more likely to develop glandular cysts in the stomach. These phenomena are due to physiological changes as a result of inhibition of the secretion of hydrochloric acid.

Ezomin, like all acid-lowering drugs, can lead to 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 with long-term therapy.

It should be used with caution in severe hepatic impairment. Dose adjustment may be required.

Use with caution in severe renal failure. Dose adjustment may be required.

With the use of proton pump inhibitors, especially when used in high doses and for an extended period (> 1 year), the risk of fractures of the femoral neck, wrist bones and vertebrae increases, especially in elderly patients.

Influence on the ability to drive vehicles and mechanisms

Due to the fact that dizziness, blurred vision and drowsiness may occur during drug therapy, care should be taken when driving vehicles and other mechanisms.

Application during pregnancy and during breastfeeding

Due to the fact that dizziness, blurred vision and drowsiness may occur during drug therapy, care should be taken when driving vehicles and other mechanisms.

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 reduce plasma concentrations and the clinical efficacy of itraconazole and ketoconazole.

It is possible with the simultaneous use of an increase in plasma concentrations of diazepam and phenytoin, which, apparently, has 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, the absorption of which depends on the acidity of the environment.

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

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

There is evidence that the combined use of esomeprazole with clarithromycin, which inhibits the CYP3A4 isoenzyme, leads to a 2-fold increase in the AUC value of esomeprazole. Concomitant use of esomeprazole and a combined inhibitor of CYP3A4 and CYP2C19 isoenzymes, for example, voriconazole, can lead to a more than 2-fold increase in the AUC value for esomeprazole.

Medicines that induce CYP2C19 and CYP3A4 isoenzymes, such as rifampicin and St. John's wort preparations, when used together with esomeprazole, can lead to a decrease in the concentration of esomeprazole in the blood plasma by accelerating its metabolism.

Side effect

From the gastrointestinal tract: abdominal pain, constipation, diarrhea, flatulence, nausea / vomiting, dry mouth.

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

Skin and subcutaneous tissue disorders: dermatitis, itching, rash, urticaria, alopecia, photosensitivity, reactions at the injection site, 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 side of 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 indicated in the instructions are aggravated, or you notice any other side effects not listed in the instructions, inform your doctor.

Overdose

Symptoms: General weakness and gastrointestinal symptoms.

Treatment: symptomatic therapy. The specific antidote is unknown. With the help of dialysis, it is poorly excreted.

Storage conditions

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

Keep out of the reach of children!

Shelf life

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

Vacation conditions

Dispensed by prescription.

Release form

1 bottle with instructions for use in a cardboard box.