Omez lyophilisate for infusion 40mg, No. 1

• peptic ulcer of the stomach and duodenum (including prevention of relapse);

• reflux esophagitis;

• hypersecretory conditions (Zollinger-Ellison syndrome, stress gastrointestinal ulcers, polyendocrine adenomatosis, systemic mastocytosis);

• NSAID gastropathy;

• prevention of aspiration of acidic stomach contents into the airways during general anesthesia (Mendelssohn's syndrome).

In severe exacerbation of peptic ulcer disease, reflux esophagitis and NSAID gastropathy , in patients who are not indicated for oral administration of the drug, the recommended daily dose of OmezЃ is 40 mg for administration in the form of an intravenous infusion.

In Zollinger-Ellison syndrome, the drug is prescribed at an initial dose of 60 mg / day. The dose should be selected individually, possibly in higher doses (80-120 mg / day). If the daily dose is over 60 mg, it should be divided into 2-3 infusions during the day.

In Mendelssohn's syndrome, the drug is prescribed at night at a dose of 40 mg and at least 2 hours before anesthesia / surgery at a dose of 40 mg.

In elderly patients, there is no need to adjust the dose.

Rules for the preparation of an infusion solution

The solution for intravenous infusion is prepared immediately before use. To prepare a solution for intravenous infusion, use only 5% dextrose (glucose) solution without preservatives. To dissolve 40 mg of lyophilized omeprazole powder, at least 5 ml of solvent are added to the vial and gently shaken until the lyophilisate is completely dissolved. The prepared solution containing 40 mg of omeprazole is diluted before administration in 100 ml of 5% dextrose (glucose) solution without preservatives for intravenous infusion for at least 30 minutes. Before injection, make sure that there are no suspended particles in the solution. The chemical and physical stability of the prepared omeprazole solution is observed within 6 hours from the moment of dissolution of omeprazole in 5% dextrose (glucose) solution.

Active ingredient: omeprazole - 40 mg

Excipients : sodium hydroxide - 5.28 mg, disodium edetate - 1 mg.

• childhood;

• pregnancy;

• lactation period;

• hypersensitivity to the drug.

The drug should be prescribed with caution in case of renal and / or hepatic insufficiency.

Lyophilisate for the preparation of a solution for infusion in the form of a homogeneous porous cake or parts thereof, or in the form of a white or almost white powder.

Clinical and pharmacological group: N + -K + -ATPase inhibitor. Antiulcer drug

Pharmaco-therapeutic group: Proton pump inhibitor

pharmachologic effect

Antiulcer drug, specific proton pump inhibitor. Inhibits the activity of H + -K + -ATPase in parietal cells of the stomach, blocking the final stage of the secretion of hydrochloric acid, thereby reducing acid production. Reduces basal and stimulated secretion regardless of the nature of the stimulus.

Omeprazole is a prodrug and is activated in the acidic environment of the secretory tubules of the parietal cells of the stomach.

The antisecretory effect after taking a dose of 20 mg occurs within the first hour, the maximum effect is after 2 hours. Inhibition of 50% of the maximum secretion lasts 24 hours.

A single dose per day provides a quick and effective suppression of daytime and nocturnal gastric secretion, reaching its maximum after 4 days of treatment and disappearing by the end of 3 to 4 days after the end of the intake.

In patients with duodenal ulcer, taking 20 mg of omeprazole maintains the pH in the stomach at 3 for 17 hours.

Pharmacokinetics

Distribution and metabolism

Binds to plasma proteins by 90-95% (albumin and acid alpha-glycoprotein).

It is almost completely metabolized in the liver with the participation of the cytochrome P450 enzyme system with the formation of 6 pharmacologically inactive metabolites (including hydroxyomeprazole, sulfide and sulfone derivatives). A significant part of the metabolism of omeprazole depends on the polymorphically expressed specific isoform CYP2C19 (S-mephenytoin hydroxylase), which is responsible for the formation of hydroxyomeprazole, the main plasma metabolite. It is an inhibitor of the isoenzyme CYP2C19.

Withdrawal

T1 / 2 for the final phase of AUC after intravenous administration of omeprazole is approximately 40 minutes (with hepatic failure - 3 hours); total plasma clearance is 0.3 to 0.6 l / min. There is no change in T1 / 2 during treatment.

It is excreted in the urine (70-80%) and in the bile (20-30%).

Pharmacokinetics in special clinical situations

In chronic renal failure, excretion decreases in proportion to the decrease in creatinine clearance.

In elderly patients, excretion decreases, bioavailability increases.

Indications

• peptic ulcer of the stomach and duodenum (including prevention of relapse);

• reflux esophagitis;

• hypersecretory conditions (Zollinger-Ellison syndrome, stress gastrointestinal ulcers, polyendocrine adenomatosis, systemic mastocytosis);

• NSAID gastropathy;

• prevention of aspiration of acidic stomach contents into the airways during general anesthesia (Mendelssohn's syndrome).

Dosage regimen

In severe exacerbation of peptic ulcer disease, reflux esophagitis and NSAID gastropathy , in patients who are not indicated for oral administration of the drug, the recommended daily dose of OmezЃ is 40 mg for administration in the form of an intravenous infusion.

In Zollinger-Ellison syndrome, the drug is prescribed at an initial dose of 60 mg / day. The dose should be selected individually, possibly in higher doses (80-120 mg / day). If the daily dose is over 60 mg, it should be divided into 2-3 infusions during the day.

In Mendelssohn's syndrome, the drug is prescribed at night at a dose of 40 mg and at least 2 hours before anesthesia / surgery at a dose of 40 mg.

In elderly patients, there is no need to adjust the dose.

Rules for the preparation of an infusion solution

The solution for intravenous infusion is prepared immediately before use. To prepare a solution for intravenous infusion, use only 5% dextrose (glucose) solution without preservatives. To dissolve 40 mg of lyophilized omeprazole powder, at least 5 ml of solvent are added to the vial and gently shaken until the lyophilisate is completely dissolved. The prepared solution containing 40 mg of omeprazole is diluted before administration in 100 ml of 5% dextrose (glucose) solution without preservatives for intravenous infusion for at least 30 minutes. Before injection, make sure that there are no suspended particles in the solution. The chemical and physical stability of the prepared omeprazole solution is observed within 6 hours from the moment of dissolution of omeprazole in 5% dextrose (glucose) solution.

Side effect

From the hematopoietic system: in some cases - leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.

From the digestive system: diarrhea or constipation, abdominal pain, nausea, vomiting, flatulence; rarely - increased activity of liver enzymes, taste disturbances; in some cases - dry mouth, stomatitis, in patients with previous severe liver disease - hepatitis (including jaundice), liver dysfunction.

From the side of the central nervous system: in patients with severe concomitant somatic diseases - dizziness, headache, agitation, depression; in patients with previous severe liver disease - encephalopathy.

From the musculoskeletal system: in some cases - arthralgia, myasthenia gravis, myalgia.

Dermatological reactions: rarely - skin rash and / or itching; in some cases - photosensitivity, exudative erythema multiforme, alopecia.

Allergic reactions: urticaria, angioedema, fever, bronchospasm, interstitial nephritis and anaphylactic shock.

Others: rarely - gynecomastia, malaise, visual impairment, peripheral edema, increased sweating, the formation of gastric glandular cysts during long-term treatment (a consequence of inhibition of the secretion of hydrochloric acid, is benign, reversible).

Contraindications for use

• childhood;

• pregnancy;

• lactation period;

• hypersensitivity to the drug.

The drug should be prescribed with caution in case of renal and / or hepatic insufficiency.

Application during pregnancy and lactation

The use of the drug OmezЃ during pregnancy and lactation (breastfeeding) is contraindicated.

Application for violations of liver function

The drug should be prescribed with caution in liver failure.

Application for impaired renal function

The drug should be prescribed with caution in case of renal failure.

Application in children

Prescription for children is contraindicated.

Use in elderly patients

In elderly patients, there is no need to adjust the dose.

special instructions

Before starting therapy, it is necessary to exclude the presence of a malignant process (especially with a stomach ulcer), because treatment, masking the symptoms, can delay the correct diagnosis.

Influence on the ability to drive vehicles and use mechanisms

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Overdose

According to clinical studies, with intravenous administration of omeprazole at a dose of up to 270 mg / day and at a dose of up to 650 mg for 3 days, dose-dependent side effects were not identified.

Symptoms: confusion, blurred vision, drowsiness, dry mouth, headache, nausea, tachycardia, arrhythmia.

Treatment: symptomatic. Hemodialysis is not effective enough.

Drug interactions

With the simultaneous use of OmezЃ can reduce the absorption of ampicillin esters, iron salts, itraconazole and ketoconazole, because omeprazole raises the pH of the stomach.

As an inhibitor of cytochrome P450, omeprazole can increase the concentration and reduce the excretion of diazepam, indirect anticoagulants (warfarin), phenytoin (drugs metabolized in the liver with the participation of CYP2C19), which in some cases may require a reduction in doses of these drugs.

At the same time, long-term use of omeprazole at a dose of 20 mg 1 time / day in combination with caffeine, theophylline, piroxicam, diclofenac, naproxen, metoprolol, propranolol, ethanol, cyclosporine, lidocaine, quinidine and estradiol did not lead to a change in their plasma concentration.

Plasma concentrations of omeprazole and clarithromycin increase during joint oral administration of these drugs, while there is no evidence of the interaction of omeprazole with metronidazole and amoxicillin.

Storage conditions

List B. The drug should be stored in a dry, dark place, out of the reach of children, at a temperature not exceeding 25 ? C.

Shelf life

Shelf life is 2 years.

Terms of sale

The drug is available with a prescription.