Omez lyophilizate solution for infusion 40mg vials, 1pc

Composition

Each bottle contains: Active ingredient: omeprazole 40 mg. Auxiliary substances:  sodium hydroxide 5.28 mg, disodium edetate 1.00 mg

Pharmacological action

Pharmacodynamics pecific proton pump inhibitor: inhibits the activity of H+/K+ – ATPASE in the parietal cells of the stomach, blocking the final stage of hydrochloric acid secretion, 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 effect is dose-dependent and provides effective inhibition of both basal and stimulated acid secretion, regardless of the nature of the stimulating factor. The antisecretory effect after taking 20 mg occurs within the first hour, a maximum of 2 hours. Inhibition of 50% of the maximum secretion lasts 24 hours. A single dose per day provides rapid and effective suppression of day and night gastric secretion, reaching its maximum after 4 days of treatment and disappearing by the end of 3-4 days after the end of the intake. In patients with duodenal ulcer disease, taking 20 mg of omeprazole keeps the intragastric pH at 3 for 17 hours. During the use of drugs that reduce the secretion of gastric glands, the concentration of gastrin in the blood plasma increases. Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A increases (see the section “Special instructions”). Pharmacokinetics Plasma protein binding-90-95% (albumin and acid alpha-1-glycoprotein). The half-life (T1 / 2) for the final phase of the pharmacokinetic curve “concentration-time” in blood plasma after intravenous use of omeprazole is about 40 minutes (in hepatic insufficiency-3 hours); total plasma clearance is from 0.3 to 0.6 l / min. There is no change in the half-life during treatment. It is almost completely metabolized in the liver with the participation of the cytochrome P450 (CYP) enzyme system with the formation of six pharmacologically inactive metabolites: hydroxyomeprazole, sulfide and sulfone derivatives, and others. A significant part of omeprazole metabolism depends on the polymorphically expressed specific isoform of CYP2C19 (S-mephenytoin hydroxylase), which is responsible for the formation of hydroxyomeprazole, the main plasma metabolite. It is an inhibitor of the CYP2C19 isoenzyme. Excretion by the kidneys (70-80%) and with bile (20-30%). In chronic renal failure, excretion decreases in proportion to the decrease in creatinine clearance. In elderly patients, excretion decreases, and bioavailability increases.

Indications

As an alternative to oral therapy if it is not possible:

• if gastric ulcer and duodenal ulcer (including relapse prevention);
• with gastroesophageal reflux disease (GERD);
• if hypersecretory States (syndrome zollingerellison, stress ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis);
• for the prevention and treatment of lesions of the gastric mucosa and duodenal ulcers caused by nonsteroidal anti-inflammatory drugs (NSAIDs-gastropathy): dyspepsia, mucosal erosion, peptic ulcer;
• to prevent aspiration of acidic stomach contents into the respiratory tract during general anesthesia (Mendelssohn syndrome).

Use during pregnancy and lactation

The use of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus. During lactation, you should stop breastfeeding.

Contraindications

Hypersensitivity to omeprazole, substituted benzimidazoles or other components of the drug. Sucrose/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption (due to the presence of sucrose in the preparation). Concomitant use with erlotinib, posaconazole, nelfinavir and atazanavir. Omeprazole is contraindicated in children, except for the following indications: gastroesophageal reflux disease for children over 2 years of age and duodenal ulcer caused by Helicobacter pylori for children over 4 years of age (see the section “Dosage and use”). Before using the drug, you should consult your doctor in the following cases: :

• in the presence of a previously diagnosed peptic ulcer of the stomach; severe liver disease, accompanied by hepatic insufficiency; renal failure; jaundice; previous surgery on the gastrointestinal tract;
• in the presence of “alarm” symptoms: significant spontaneous reduction of body weight, repeated vomiting, vomiting blood, change in color of stool (black, tar-like stool – melena), impaired swallowing;
• the appearance of new symptoms or modification of already existing symptoms of the gastrointestinal tract;
• while the use of one or more of the following drugs: clopidogrel, digoxin, ketoconazole, Itraconazole, warfarin, Cilostazol, diazepam, phenytoin, saquinavir, tacrolimus, clarithromycin, voriconazole, rifampin, St. John’s wort preparations (see section “Interaction with other medicines”).

Osteoporosis. Although a causal relationship between omeprazole use and osteoporotic fractures has not been established, patients at risk of developing osteoporosis or osteoporotic fractures should be under appropriate clinical supervision.

Side effects

The frequency of adverse drug reactions is described in accordance with the following gradation: very common (>1/10); common (≥1/100, ><1/10); infrequent (≥1/1000, <1/100); rare (≥1/10000, <1/1000); very rare (Skin and subcutaneous tissue disorders: infrequently-dermatitis, pruritus, skin rash, urticaria; rarely-alopecia, photosensitivity reactions, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis. Musculoskeletal and connective tissue disorders: infrequently-fractures of the hip, wrist bones, vertebrae; rarely-arthralgia, myalgia, muscle weakness. Nervous system disorders: often-headache; infrequently-dizziness, paresthesia, drowsiness; rarely-taste disorders. Mental disorders: infrequently-insomnia; rarely – increased excitability, aggressiveness, impaired consciousness, depression, hallucinations. Gastrointestinal disorders: often-abdominal pain, constipation, diarrhea, flatulence, nausea, vomiting; rarely-dry mouth, stomatitis, gastrointestinal candidiasis, microscopic colitis. Liver and biliary tract disorders: infrequently-increased activity of “liver” enzymes; rarely-hepatitis with / without jaundice, liver failure, encephalopathy in patients with previous severe liver diseases. Genital and breast disorders: rarely-gynecomastia. Blood and lymphatic system disorders: leukopenia, thrombocytopenia, agranulocytosis, pancytopenia. Immune system disorders: rarely – hypersensitivity reactions: fever, angioedema, anaphylactic reaction / anaphylactic shock. Respiratory, thoracic and mediastinal disorders: rarely-bronchospasm. Renal and urinary tract disorders: rarely-interstitial nephritis. Hearing disorders and labyrinth disorders: infrequently-vertigo. Visual disturbances: rarely – blurred vision. Metabolic and nutritional disorders: rarely-hyponatremia; very rarely-hypomagnesemia, hypocalcemia due to severe hypomagnesemia, hypokalemia due to hypomagnesemia. General disorders: infrequently-malaise; rarely-increased sweating, peripheral edema.

Interaction

Long-term use of omeprazole at a dose of 20 mg once a day in combination with caffeine, theophylline, piroxicam, diclofenac, naproxen, metoprolol, propranolol, ethanol, cyclosporine, lidocaine, quinidine and estradiol did not lead to changes in their plasma concentrations. There was no interaction with concomitant antacids. Changes the bioavailability of any drug whose absorption depends on the pH value (for example, iron salts).

How to take, course of use and dosage

Omez® is administered intravenously for 20-30 minutes. It is recommended to introduce the infusion solution immediately after its preparation. Doses are selected individually, sometimes a higher dose is required. If the daily dose exceeds 60 mg, the dose should be divided into two doses. As an alternative to oral therapy if it is not possible: for gastric and duodenal ulcers (including relapse prevention), it is recommended to administer an infusion of Omez® at a dose of 40 mg once a day; for gastroesophageal reflux disease (GERD), an infusion of Omez® at a dose of 40 mg once a day is recommended;for hypersecretory conditions (Zollinger-Ellison syndrome, stress ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis), an initial intravenous use of Omez® at a dose of 60 mg per day is recommended;for the prevention and treatment of damage to the gastric and duodenal mucosa in patients with non-steroidal anti – inflammatory drugs (NSAIDs)-gastropathy (dyspepsia, mucosal erosion, peptic ulcer), it is recommended to prescribe an infusion of Omez® at a dose of 40 mg once a day.To prevent aspiration of acidic stomach contents into the respiratory tract during general anesthesia (Mendelssohn syndrome), the drug is prescribed the night before at a dose of 40 mg and at least 2 hours before anesthesia / surgery at a dose of 40 mg. After the end of parenteral therapy, antisecretory therapy with oral dosage forms (for example, omeprazole 40 mg once a day for 4 weeks) is recommended to suppress acid secretion. Use of the drug in special cases of impaired renal function. No dose adjustment is required. Impaired liver function. In patients with impaired liver function, the bioavailability and clearance of omeprazole are increased. In this regard, the therapeutic dose should not exceed 20 mg per day. Advanced age. The metabolic rate of omeprazole decreases in the elderly, but no dose adjustment is required. Instructions for preparing the infusion solutionthe infusion solution is prepared by dissolving lyophilized omeprazole powder in 100 ml of 5% dextrose (glucose) solution for infusions or in 100 ml of saline infusion solution. A 5% dextrose (glucose) infusion solution should be used within 6 hours. The saline infusion solution should be used within 12 hours. Before use, make sure that there are no suspended particles in the solution. Preparation of the solution for infusions in vials 1. Use a syringe to collect 5 ml of the solution for infusions from the vial. 2. Introduce the infusion solution into the vial with lyophilized omeprazole powder, shake the vial until the drug is completely dissolved. 3. Fill the syringe with omeprazole solution. 4. Transfer the omeprazole solution to the vial. 5. Repeat operations 1-4 to transfer the entire drug from the vial. Preparation of the infusion solution in a soft container 1. Use a double-sided needle (adapter) to prepare the infusion solution. Use one end of the needle to pierce the membrane of the infusion bag, and connect the other end of the needle to a vial of lyophilized omeprazole. 2. Dissolve the omeprazole powder by pumping the infusion solution from the bag to the vial and back. 3. Make sure that the powder is completely dissolved, then disconnect the empty bottle and remove the needle from the infusion bag.

Overdose

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

Treatment: symptomatic. Hemodialysis is not effective enough.

Special instructions

If a stomach ulcer is suspected in the early stages, it is necessary to undergo an X-ray or endoscopic examination to establish the correct diagnosis and prescribe adequate treatment. In the presence of any alarming symptoms, such as significant spontaneous weight loss, frequent vomiting, dysphagia, vomiting with blood or melena, as well as in the presence of a stomach ulcer (or if a stomach ulcer is suspected), the possibility of malignancy should be excluded, since treatment with Omez® may smooth out the symptoms and delay the diagnosis. Patients at risk of developing osteoporosis or fractures associated with it should be under appropriate clinical supervision, although a causal relationship between the use of omeprazole/esomeprazole and fractures associated with osteoporosis has not been established. Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (CgA) increases. An increase in the concentration of CgA in blood plasma may affect the results of examinations for the detection of neuroendocrine tumors. To prevent this effect, therapy with proton pump inhibitors should be suspended 5 days before the CgA concentration study. If the CgA concentration has not returned to normal during this time, the study should be repeated. During treatment with omeprazole, dizziness, drowsiness, and visual impairment may occur, so caution should be exercised when driving vehicles and performing other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Storage conditions

In a place protected from light at a temperature not exceeding 25 ° C. Keep out of reach of children!

Shelf life

2 years

Active ingredient

Omeprazole

Conditions of release from pharmacies

By prescription

Dosage form

solution for infusions

Purpose

For adults as directed by your doctor

Indications

Stomach and Duodenal ulcers, Heartburn, GI infections caused by Helicobacter Pylori, Reflux Esophagitis