Esomeprazole tablets 40mg, No. 28

Gastroesophageal reflux disease: erosive reflux esophagitis (treatment), prevention of relapse in patients with healed esophagitis, symptomatic treatment of GERD.

As part of combination therapy: eradication of Helicobacter pylori, duodenal ulcer associated with Helicobacter pylori, prevention of recurrence of peptic ulcers in patients with peptic ulcer associated with Helicobacter pylori.

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

It is taken internally. The dose is 20-40 mg 1 time / day. The duration of admission depends on the indications, treatment regimen, effectiveness.

In severe hepatic impairment, the maximum dose is 20 mg / day.

Active ingredient: esomeprazole magnesium dihydrate - 43.4 mg, which corresponds to the content of esomeprazole - 40 mg

Excipients : low-substituted hyprolose (hydroxypropyl cellulose), pregelatinized corn starch, colloidal silicon dioxide, mannitol, sodium stearyl fumarate, microcrystalline cellulose type 200, sodium carboxymethyl starch.

Shell composition: hypromellose, macrogol - 6000, acrylysis II yellow 493Z220000 (methacrylic acid and ethyl acrylate copolymer (1: 1), talc, titanium dioxide, poloxamer 407, calcium silicate, sodium bicarbonate, iron dye yellow oxide, sodium lauryl sulfate).

Lactation period, hypersensitivity to esomepromazole.

Trade name: Esomeprazole

International non-proprietary name of the drug: esomeprazole

Dosage form:

enteric film-coated tablets

Composition:

Active ingredient: esomeprazole magnesium dihydrate - 43.4 mg, which corresponds to the content of esomeprazole - 40 mg

Excipients : low-substituted hyprolose (hydroxypropyl cellulose), pregelatinized corn starch, colloidal silicon dioxide, mannitol, sodium stearyl fumarate, microcrystalline cellulose type 200, sodium carboxymethyl starch.

Shell composition: hypromellose, macrogol - 6000, acrylysis II yellow 493Z220000 (methacrylic acid and ethyl acrylate copolymer (1: 1), talc, titanium dioxide, poloxamer 407, calcium silicate, sodium bicarbonate, iron dye yellow oxide, sodium lauryl sulfate).

Clinical and pharmacological group: N + -K + -ATPase inhibitor

Pharmaco-therapeutic group: Stomach glands secretion lowering agent - proton pump inhibitor

pharmachologic effect

H + -K + -ATPase 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 medium of the secretory tubules of the 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 / day, the average maximum concentration of hydrochloric acid after stimulation with pentagastrin decreases by 90%.

Pharmacokinetics

Unstable in an acidic environment. In vivo, only a small fraction of esomeprazole is converted to the R isomer. After oral administration, it is rapidly absorbed from the gastrointestinal tract. Cmax in blood plasma is achieved after 1-2 hours. Absolute bioavailability with repeated administration at a dose of 20 mg 1 time / day is 89%. Vd - 0.22 l / kg. Plasma protein binding - 97%. It is completely metabolized with the participation of isoenzymes of the cytochrome P450 system. The main part is metabolized with the participation of CYP2C19 with the formation of hydroxy- and demethylated metabolites of esomeprazole. The rest of the metabolism is carried out by another isoenzyme CYP3A4; in this case, the sulfo-derivative of esomeprazole is formed, which is the main metabolite determined in plasma. All metabolites are pharmacologically inactive.In patients with an active CYP2C19 isoenzyme (patients with an active metabolism), the systemic clearance is 17 l / h after a single dose and 9 l / h after multiple doses. T1 / 2 - 1.3 hours with systematic administration in a dosing regimen 1 time / day. AUC increases with repeated administration (non-linear dose and AUC dependence 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 sulfonated metabolite). Does not cumulate. Up to 80% of the dose is excreted in the form of metabolites by the kidneys (less than 1% - unchanged), the rest - with bile.AUC increases with repeated administration (non-linear dose and AUC dependence 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 sulfonated metabolite). Does not cumulate. Up to 80% of the dose is excreted in the form of metabolites by the kidneys (less than 1% - unchanged), the rest - with bile.AUC increases with repeated administration (non-linear dose and AUC dependence 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 sulfonated metabolite). Does not cumulate. Up to 80% of the dose is excreted in the form of metabolites by the kidneys (less than 1% - unchanged), the rest - with bile.Up to 80% of the dose is excreted in the form of metabolites by the kidneys (less than 1% - unchanged), the rest - with bile.Up to 80% of the dose is excreted in the form of metabolites by the kidneys (less than 1% - unchanged), the rest - with bile.

In patients with inactive metabolism (1-2%), the metabolism of esomeprazole is mainly carried out with the participation of the CYP3A4 isoenzyme. When taken systematically at a dose of 40 mg 1 time / day, the average AUC is 100% higher than the value of this parameter in patients with active metabolism. Average Cmax values ??in plasma in patients with inactive metabolism are increased by about 60%.

In severe hepatic insufficiency, the metabolic rate is reduced, which is accompanied by a 2-fold increase in AUC.

Indications

Gastroesophageal reflux disease: erosive reflux esophagitis (treatment), prevention of relapse in patients with healed esophagitis, symptomatic treatment of GERD.

As part of combination therapy: eradication of Helicobacter pylori, duodenal ulcer associated with Helicobacter pylori, prevention of recurrence of peptic ulcers in patients with peptic ulcer associated with Helicobacter pylori.

Dosage regimen

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

It is taken internally. The dose is 20-40 mg 1 time / day. The duration of admission depends on the indications, treatment regimen, effectiveness.

In severe hepatic impairment, the maximum dose is 20 mg / day.

Side effect

Often: headache, abdominal pain, diarrhea, flatulence, nausea, vomiting, constipation.

Rarely: dermatitis, itching, hives, dizziness, dry mouth.

Contraindications for use

Lactation period, hypersensitivity to esomepromazole.

Application during pregnancy and lactation

There are no data on the safety of using esomeprazole during pregnancy. Application is possible in cases where the expected benefit of therapy for the mother outweighs the possible risk to the fetus.

In experimental studies in animals have not revealed any direct or indirect negative impact on the development of the embryo or fetus. The administration of the racemic substance also did not have any negative effect on animals during pregnancy, during childbirth, as well as during postnatal development.

Contraindicated during lactation.

Application for violations of liver function

In severe hepatic impairment, the maximum dose is 20 mg / day.

special instructions

In the presence of symptoms such as significant spontaneous weight loss, frequent vomiting, dysphagia, vomiting of blood or melena, and in the presence (or suspicion) of a stomach ulcer, the possibility of a malignant neoplasm should be excluded, since treatment with esomeprazole can lead to a reduction 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 who take 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.

Drug interactions

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

It is believed that with simultaneous use, it is possible to reduce plasma concentrations and the clinical efficacy of itraconazole and ketoconazole.

With simultaneous use with clarithromycin, a case has been described of a significant increase in the AUC of esomeprazole due to the inhibition of its metabolism under the influence of clarithromycin.

With simultaneous use, it is possible to increase the plasma concentrations of diazepam and phenytoin, which, apparently, has no clinical significance.

Storage
conditions Store in a dry, dark place at a temperature not exceeding 25 ? C.
Keep out of the reach of children.

Shelf life is
2 years.
Do not use after the expiration date.

Dispensing conditions
Prescription