Omez - instructions for use, dose, side effects, contraindications

Specific inhibitor of the proton pump: inhibits the activity of H⁺/TO⁺-ATPase in parietal cells of the stomach, blocking the final stage of secretion of hydrochloric acid, thereby reducing acid production. Reduces basal and stimulated secretion irrespective of the nature of the stimulus.

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

The effect is dose-dependent and provides an 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 after 2 hours. Inhibition of 50% of 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 admission. In patients with duodenal ulcer, taking 20 mg of omeprazole maintains an intragastric pH at level 3 for 17 hours.

During the use of drugs that reduce the secretion of the glands of the stomach, the concentration of gastrin in the blood plasma increases. Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (see section "Special instructions").

Pharmacokinetics:

The connection with plasma proteins is 90-95% (albumin and acid alpha-1 glycoprotein).

Half-life (T_1/2) for the final phase of the pharmacokinetic curve "concentration-time" in blood plasma after intravenous administration of omeprazole is about 40 minutes (with hepatic insufficiency - 3 hours); the total plasma clearance is from 0.3 to 0.6 l / min. Changes in the value of the half-life during treatment do not occur.

Almost completely metabolized in the liver with the participation of the enzymatic system of cytochrome R₄₅₀ (CYP) with the formation of six pharmacologically inactive metabolites: hydroxyomeprazole, sulfide and sulphonic derivatives and others.

A significant portion of the metabolism of omeprazole depends on the polymorphically expressed specific isoform CYP2C19 (S-mephenytoin hydroxylase), responsible for the formation of hydroxyomeprazole, the main plasma metabolite. Is an inhibitor of isoenzyme CYP2C19.

Kidney excretion (70-80%) and with bile (20-30%). In chronic renal failure, excretion decreases in proportion to a decrease in creatinine clearance. In elderly patients excretion decreases, bioavailability increases.

Indications:

As an alternative to oral therapy when it is not possible to conduct:

- with peptic ulcer of stomach and duodenum (including, prevention of relapses);

- with gastroesophageal reflux disease (GERD);

- at hypersecretory conditions (Zollinger-Ellison syndrome, stress ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis);

- for the prevention and treatment of damage to the mucous membrane of the stomach and duodenum,caused by the use of non-steroidal anti-inflammatory drugs (NSAIDs-gastropathy): dyspepsia, erosion of the mucous membrane, peptic ulcer.- to prevent aspiration of acidic stomach contents in the respiratory tract during general anesthesia (Mendelssohn syndrome).

Contraindications:

Hypersensitivity to omeprazole or other components of the drug.

Simultaneous reception with erlotinib, posaconazole, nelfinavir and atazanavir. Breastfeeding period. Children under 18 years of age (efficacy and safety not established for this dosage form).

Carefully:

Renal failure (correction of the dose of omeprazole is not required).

Hepatic insufficiency (see section "Method of administration and dosing regimen").

Pregnancy.

Simultaneous use with clopidogrel, itraconazole, warfarin, cilostazol, diazepam, phenytoin, saquinavir, tacrolimus, clarithromycin, voriconazole, rifampicin, preparations of St. John's wort perfumed.

Osteoporosis. Although the cause-and-effect relationship of omeprazole with fractures against osteoporosis is not established, patients with a risk of developing osteoporosis or fractures against it should be under appropriate clinical supervision.

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.

Lactation should stop breastfeeding.

Dosing and Administration:

The drug Omega® is administered intravenously for 20-30 minutes. It is recommended to inject the solution for infusion 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 when it is not possible to conduct:

- with peptic ulcer of the stomach and duodenum (including the prevention of relapses) it is recommended to prescribe an infusion of Omez ® in a dose of 40 mg once a day;

- in gastroesophageal reflux disease (GERD), it is recommended to prescribe an infusion of Omez ® in a dose of 40 mg once a day;

- at hypersecretory states (Zollinger-Ellison syndrome,stress ulcers of the gastrointestinal tract, polyendocrine adenomatosis, systemic mastocytosis), an initial intravenous injection of Omez® in a dose of 60 mg per day is recommended;

- for the prevention and treatment of gastric and duodenal ulcer damage caused by the use of non-steroidal anti-inflammatory drugs - NSAIDs-gastropathy (dyspepsia, erosion of the mucous membrane, peptic ulcer), it is recommended to prescribe an infusion of Omez® in a dose of 40 mg once a day.

To prevent aspiration of acidic stomach contents in the respiratory tract during general anesthesia (Mendelssohn syndrome) the drug is prescribed overnight at a dose of 40 mg and at least 2 hours before anesthesia / surgery at a dose of 40 mg. After the completion of parenteral therapy to suppress acid secretion, antisecretory therapy with oral dosage forms is recommended (for example, omeprazole 40 mg once a day for 4 weeks).

Application of the drug in special cases

Impaired renal function. Correction of the dose is not required.

Violation of the function of the liver. In patients with impaired liver function, bioavailability and omeprazole clearance are increased. In this regard, the therapeutic dose should not exceed 20 mg per day.

Elderly age. The rate of metabolism of omeprazole in elderly people is reduced, but dose adjustment is not required.

Instructions for preparing a solution for infusions

Solution for infusion is prepared by dissolving the lyophilized powder of omeprazole in 100 ml 5% solution of dextrose (glucose) for infusion or in 100 ml infusion physiological solution.

Solution for infusions on 5% dextrose (glucose) should be used within 6 hours. The infusion solution in physiological saline should be used within 12 hours. Before the introduction, it should be ensured that there are no suspended particles in the solution.

Preparation of a solution for infusions in vials

1. Draw 5 ml of the infusion solution from the vial with a syringe.

2. Introduce the infusion solution into a vial of lyophilized omeprazole powder, shake the vial until the drug dissolves completely.

3. Draw a syringe solution of omeprazole.

4. Transfer the solution of omeprazole to the vial.

5. Repeat steps 1-4 in order to transfer the entire preparation from the vial.

Preparation of a solution for infusions in a soft container

1. To prepare a solution for infusions, use a two-sided needle (transitional).With one end of the needle, pierce the membrane of the infusion bag, and connect the other end of the needle to the vial of lyophilized omeprazole.

2. Dissolve the powder of omeprazole by pumping the infusion solution from the bag into the vial and back.

3. Make sure that the powder is completely dissolved, then disconnect the empty vial and remove the needle from the infusion bag.

Side effects:

The frequency of unwanted drug reactions is set out in accordance with the following gradation: very often (> 1/10); often (≥1/100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10000, <1/1000); very rarely (<1/10000, including single cases).

Disturbances from the skin and subcutaneous tissues: rarely dermatitis, itchy skin, skin rash, hives; rarely - alopecia, photosensitivity reactions, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis.

Disturbances from musculoskeletal and connective tissue: infrequently - fractures of the thigh, bones of the wrist, vertebrae; rarely - arthralgia, myalgia, muscle weakness.

Disturbances from the nervous system: often - headache; infrequently - dizziness, paresthesia, drowsiness; rarely - a taste disorder.

Disorders of the psyche: infrequently - insomnia; rarely - increased excitability, aggressiveness, impaired consciousness, depression, hallucinations.

Disorders from the gastrointestinal tract: often - abdominal pain, constipation, diarrhea, flatulence, nausea, vomiting; rarely - dry mouth, stomatitis, gastrointestinal candidiasis, microscopic colitis.

Disturbances from the liver and bile ducts: infrequently - increased activity of "hepatic" enzymes; rarely - hepatitis with / without jaundice, liver failure, encephalopathy in patients with previous severe liver disease.

Violations of the genitals and breast: rarely - gynecomastia.

Violations from the blood and lymphatic system: leukopenia, thrombocytopenia, agranulocytosis, pancytopenia. Immune system disorders: rarely - hypersensitivity reactions: fever, angioedema, anaphylactic reaction / anaphylactic shock.

Disturbances from the respiratory system, chest and mediastinal organs: rarely - bronchospasm.

Disorders from the kidneys and urinary tract: rarely interstitial nephritis.

Hearing disorders and labyrinthine disturbances: infrequently - vertigo.

Disturbances on the part of the organ of sight: rarely - blurred vision.

Disorders from the metabolism and nutrition: rarely - hyponatremia; very rarely - hypomagnesemia, hypocalcemia due to severe hypomagnesemia, hypokalemia due to hypomagnesemia.

General disorders: infrequently - malaise; rarely - increased sweating, peripheral edema.

Overdose:

According to clinical studies with intravenous administration of up to 270 mg of the drug per day and in a dose of up to 650 mg in three days, dose-dependent side effects were not detected. Symptoms: confusion, blurred vision, drowsiness, dry mouth, headache, nausea, tachycardia, arrhythmia.

Treatment: symptomatic. Hemodialysis is not effective enough.

Interaction:The decrease in the secretion of hydrochloric acid in the stomach in the treatment with omeprazole and other inhibitors of the proton pump can lead to a decrease or increase in the absorption of other drugs, the absorption of which depends on the acidity of the medium. Like other drugs that reduce the acidity of gastric juice,treatment with omeprazole may lead to a decrease in absorption of ketoconazole, itraconazole, posaconazole, erlotinib, iron preparations and cyanocobalamin. They should be avoided together with omeprazole.

The bioavailability of digoxin when used concomitantly with omeprazole is increased by 10% (correction of the digoxin dosage regimen may be required). Care should be taken when using these drugs at the same time in elderly patients.

With simultaneous application with omeprazole, an increase in plasma concentration and an increase in the half-life of warfarin, diazepam, phenytoin, cilostazol, imipramine, clomipramine, citalopram, hexobarbital, disulfiram, as well as other drugs metabolized in the liver with the participation of isoenzyme CYP2C19 (a reduction in the doses of these drugs may be required).

It was shown that omeprazole interacts with some antiretroviral drugs. The mechanisms and the clinical significance of these interactions are not always known. An increase in pH on the background of omeprazole therapy may affect the absorption of antiretroviral drugs. It is also possible to interact at the isoenzyme level CYP2C19. When combined use of omeprazole and some antiretroviral drugs, such as atazanavir and nelfinavir, against the background of therapy with omeprazole there is a decrease in their concentration in serum. When used simultaneously with omeprazole, the area under the pharmacokinetic concentration-time curve of atazanavir decreases by 75%. In this regard, the joint use of omeprazole with antiretroviral drugs, such as atazanavir and nelfinavir, is contraindicated.

With the simultaneous use of omeprazole with clopidogrel, there is a decrease in the antiplatelet effect of the latter.

With the combined use of methotrexate with proton pump inhibitors, a slight increase in plasma methotrexate concentration was observed in some patients. When treating high doses of methotrexate, stop taking omeprazole temporarily.

With the simultaneous use of omeprazole and tacrolimus, an increase in tacrolimus concentration in serum was noted, which may require correction of its dose.

Simultaneous application with inhibitors of isoenzymes CYP2C19 and CYP3A4 (such as clarithromycin, erythromycin, voriconazole) can lead to an increase in the plasma concentration of omeprazole, which may require correction of the dose of omeprazole in patients with severe hepatic insufficiency in the case of its long-term use. Inductors of isoenzymes CYP2C19 and CYP3A4, such as rifampicin, preparations of St. John's wort perfumed (Hypericum perforatum), when combined with omeprazole may lead to a decrease in the concentration of omeprazole in the blood plasma due to the acceleration of the metabolism of omeprazole.

When combined with omeprazole with clarithromycin or erythromycin, the concentration of omeprazole in the blood plasma is increased.

The simultaneous administration of omeprazole with amoxicillin or metronidazole does not affect the concentration of omeprazole in the blood plasma.

There was no effect of omeprazole on antacid agents, theophylline, caffeine, quinidine, lidocaine, propranolol, ethanol.

Special instructions:If you suspect a stomach ulcer in the early stages, you need to undergo an X-ray or endoscopy examination to establish the correct diagnosis and the appointment of an adequate treatment.

In the presence of any anxiety symptoms, such as significant spontaneous weight loss, frequent vomiting, dysphagia, vomiting with blood or melena,and if there is a stomach ulcer (or if a stomach ulcer is suspected), the possibility of malignant growth should be excluded, since treatment with Omez® can lead to a smoothing of the symptoms and delay the diagnosis. Patients with a risk of developing osteoporosis or fractures against it should be under appropriate clinical supervision, although a causal relationship between omeprazole / esomeprazole and fractures against osteoporosis is not established.

Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (CgA). Increase in concentration CgA in blood plasma can influence 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 concentration test CgA. If during this time the concentration CgA did not return to normal, the study should be repeated.

Effect on the ability to drive transp. cf. and fur:During treatment with omeprazole may occur dizziness, drowsiness, impaired vision,therefore, care should be taken when driving vehicles and performing other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:Lyophilizate for solution for infusion, 40 mg.

Packaging:

The preparation in a vial of colorless transparent glass type I (Eur Ph), Closed with chlorobutyl stopper, crimped with an aluminum cap with a protective plastic cover. Each bottle, along with instructions for use, is placed in a cardboard box.

Storage conditions:

List B.

In a dry, the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children!

Shelf life:

2 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-004124/09

Date of registration:26.05.2009 / 19.02.2013

Expiration Date:Unlimited

The owner of the registration certificate:Dr. Reddy's Laboratories Ltd.Dr. Reddy's Laboratories Ltd. India

Manufacturer: & nbsp

DR. REDDY`S LABORATORIES, LTD. India

Representation: & nbspDR REDDY'S LABORATORIS LTD. DR REDDY'S LABORATORIS LTD. India

Information update date: & nbsp06.06.2017

Illustrated instructions

Instructions

Omez® (Omez®)