Gastrozole capsules 10mg, 14pcs

Composition

Omeprazole pellets – 117.5 mg, containing:

Active ingredient: omeprazole – 10.0 mg;

excipients: mannitol – 19,97 mg, sucrose – 32,11 mg, disodium hydrogen phosphate was 1.49 mg, sodium lauryl sulfate – 0,40 mg, lactose monohydrate – 4.00 mg, calcium carbonate – 4.00 mg, hypromellose (hydroxypropyl methylcellulose E-5) – of 10.28 mg methacrylic acid copolymer ethylacrylate [1: 1](L-30D) – 29,37 mg, propylene glycol – 0,95 mg, diethyl – 2,94 mg cetyl alcohol – 0,88 mg, sodium hydroxide – 0.18 mg, Polysorbate-80 – 0.35 mg, povidone (polyvinylpyrrolidone, povidone K-30) – 0.30 mg, titanium dioxide – 0.21, talc – 0.07 mg.

Composition of hard gelatin capsule shell:

body: titanium dioxide (E 171) – 2.0000%, gelatin-up to 100%.

cap: titanium dioxide (E 171) – 1.3333%, dye sunset yellow (E 110) – 0.0044%, quinoline yellow (E 104) – 0.9197%, gelatin – up to 100%.

Pharmacological action

Pharmacotherapeutic group: a means of reducing the secretion of gastric glands-proton pump inhibitor

ATX code: A 02 BC 01

Pharmacological action

Pharmacodynamics

Omeprazole inhibits the enzyme H+K+-ATPASE (“proton pump”) in the parietal cells of the stomach, thereby blocking the final stage of hydrochloric acid secretion. This leads to a decrease in basal and stimulated acid secretion, regardless of the nature of the stimulus.

After a single oral dose, the effect of omeprazole occurs within the first hour and lasts for 24 hours. The maximum effect is achieved after 2 hours. After discontinuation of the drug, secretory activity is fully restored in 3 to 5 days.

Pharmacokinetics

Suction

After oral use, omeprazole is rapidly absorbed from the gastrointestinal tract, the maximum concentration (Cmax) of omeprazole in blood plasma is reached in 0.5-3.5 hours. Bioavailability is 30-40%.

Distribution

Binding to plasma proteins is about 95%.

Metabolism

Omeprazole is almost completely metabolized in the liver with the participation of the CYP2C19 isoenzyme with the formation of six pharmacologically inactive metabolites.

Deduction

The elimination half-life (T1 / 2) is 0.5-1 hour. It is excreted as metabolites by the kidneys (70-80%) and with bile (20-30%).

Pharmacokinetics in special clinical cases

In patients with hepatic insufficiency, bioavailability increases significantly, and the elimination half-life increases to 3 hours. In elderly patients, the rate of elimination decreases, and bioavailability increases.

Indications

Symptoms of gastroesophageal reflux, such as heartburn, acid belching.

Use during pregnancy and lactation

The results of three prospective epidemiological studies (more than 1000 observations) showed that the use of omeprazole in pregnant women does not adversely affect the course of pregnancy and the health of the fetus/newborn. However, before using the drug during pregnancy, it is recommended to consult a doctor.

Omeprazole passes into breast milk. If it is necessary to use the drug during lactation, the question of stopping breast-feeding should be decided.

Contraindications

Hypersensitivity to omeprazole, substituted benzimidazoles or other components of the drug.

Concomitant use with nelfinavir, atazanavir, erlotinib, posaconazole.

Under 18 years of age.

Precautions for use

Before using the drug, you should consult your doctor in the following cases: :

— in the presence of previously diagnosed peptic ulcer of the stomach; severe liver disease, accompanied by liver failure; jaundice; previous surgery on the gastrointestinal tract;

— in the presence of “alarm” symptoms: significant spontaneous loss of body weight, repeated vomiting, vomiting blood, changes in color of stool (black, tar-like stool — melena), impaired swallowing;

— with the appearance of new symptoms or modification of already existing symptoms of the gastrointestinal tract;

— in the presence of osteoporosis;

— due to the symptomatic treatment of dyspepsia or heartburn sustainable (for 4 weeks or more);

— while the use of one or more of the following drugs: clopidogrel, digoxin, erlotinib, ketoconazole, Itraconazole, warfarin, Cilostazol, diazepam, phenytoin, saquinavir, tacrolimus, clarithromycin, voriconazole, rifampin, St. John’s wort preparations (see Interactions with other medicines).

It is also recommended to consult a doctor before using the drug Gastrozol® during pregnancy and lactation (see the section Use during pregnancy and lactation. )

Side effects

The frequency of side effects is graded as follows: very common (≥1/10); common (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rare (≥1/10000, <1/1000); very rare (

Allergic reactions: infrequently-urticaria, skin rash, pruritus; rarely-fever, urticaria, angioedema, anaphylactoid reactions; very rarely-eosinophilia.

From the gastrointestinal tract: often-nausea, vomiting, abdominal pain, diarrhea or constipation, flatulence; infrequently — increased activity of “liver” enzymes (transaminases) and alkaline phosphatase (reversible), perversion of taste (usually passes after stopping therapy); rarely — dry mouth, stomatitis, candidiasis of the gastrointestinal tract, hepatitis (with or without jaundice), microscopic colitis, discoloration of the tongue to brown — brown color. development and appearance of benign salivary gland cysts when used concomitantly with clarithromycin (the phenomena are reversible after discontinuation of therapy); very rarely-liver failure (in patients with previous severe liver disease).

From the nervous system: often-headache; infrequently-dizziness, paresthesia, drowsiness, insomnia; rarely-agitation, reversible confusion, depression; very rarely-aggression, confusion, hallucinations; against the background of severe liver disease — encephalopathy.

From the skin and subcutaneous tissues: infrequently-dermatitis; rarely-photosensitization (redness of the skin), alopecia; very rarely-erythema multiforme, Stevens-Johnson syndrome (severe erythema multiforme, characterized by the appearance of spots and blisters on the skin and mucous membranes against the background of high fever and joint pain), toxic epidermal necrolysis; frequency unknown – subacute cutaneous lupus erythematosus.

From the side of the visual organ: infrequently-visual disturbances, including a decrease in visual fields, a decrease in visual acuity and clarity (usually disappear after discontinuation of therapy).

From the side of the organ of hearing and labyrinth disorders: infrequently-auditory perception disorders, including “tinnitus” (usually disappear after stopping therapy), vertigo.

Musculoskeletal and connective tissue disorders: infrequently-fractures of the vertebrae, wrist bones, femoral head (see section “Special instructions”); rarely — myalgia (muscle pain), arthralgia (joint pain), muscle weakness.

From the respiratory system: rarely-bronchospasm.

From the side of the kidneys and urinary tract: rarely-interstitial nephritis.

Hematopoietic disorders: rarely-leukopenia, thrombocytopenia; very rarely-agranulocytosis, pancytopenia.

From the endocrine system: very rarely — gynecomastia.

Other: infrequently-peripheral edema, malaise; rarely-increased sweating, hyponatremia; very rarely-hypomagnesemia, hypocalcemia due to severe hypomagnesemia.

Cases of glandular cysts in the stomach have been reported in patients taking drugs that reduce the secretion of gastric glands for a long period of time; cysts are benign, pass on their own against the background of continuing therapy.

In case of side effects that are not specified in these instructions, you should immediately consult a doctor.

Interaction

You should consult your doctor before taking Gastrozol® if you are receiving treatment with one or more of the medications listed in this section.

Reduced secretion of hydrochloric acid in the stomach during treatment with omeprazole and other proton pump inhibitors may 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 reduce the 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 increases by 10% (it may be necessary to adjust the dosage regimen of digoxin). Caution should be exercised when concomitantly using these drugs in elderly patients.

Omeprazole has been shown to interact with some antiretroviral drugs. The mechanisms and clinical significance of these interactions are not always known. An increase in the pH value during omeprazole therapy may affect the absorption of antiretroviral drugs.

Interaction at the level of the CYP2 isoenzyme with 19 is also possible. When omeprazole is co-administered with some antiretroviral drugs, such as atazanavir and nelfinavir, a decrease in their serum concentrations is observed during omeprazole therapy.

When used concomitantly with omeprazole, the area under the concentration-time curve of atazanavir decreases by 75%. In this regard, the combined use of omeprazole with antiretroviral drugs, such as atazanavir and nelfinavir, is contraindicated.

When used concomitantly with omeprazole, there is an increase in the plasma concentration of saquinavir / ritonavir up to 70%, while the tolerability of treatment in patients with HIV infection does not worsen.

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

When used concomitantly with omeprazole, it is possible to increase the plasma concentration and increase 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 the CYP2C19 isoenzyme (it may be necessary to reduce the doses of these drugs).

Concomitant use of omeprazole and tacrolimus has been associated with increased serum concentrations of tacrolimus, which may require dose adjustment.

In some patients, an increase in the concentration of methotrexate was noted against the background of co-use with proton pump inhibitors. When prescribing high doses of methotrexate, the possibility of temporary discontinuation of omeprazole should be considered.

Concomitant use with inhibitors of the CYP2C19 and CYP3A4 isoenzymes (such as clarithromycin and voriconazole) may lead to an increase in the plasma concentration of omeprazole, which may require dose adjustment of omeprazole in patients with severe hepatic insufficiency, if it is used for a long time.

Inducers of CYP2C19 and CYP3A4 isoenzymes (for example, rifampicin, Hypericum perforatum) when used together with omeprazole can accelerate its metabolism, thereby reducing the concentration of omeprazole in blood plasma.

There was no clinically significant interaction of omeprazole with antacids, caffeine, propranolol, theophylline, metoprolol, lidocaine, quinidine, erythromycin, phenacetin, estradiol, amoxicillin, budesonide, diclofenac, metronidazole, naproxen, piroxicam.

How to take, course of use and dosage

Inside, with a sufficient amount of water (the contents of the capsule can not be chewed),30 minutes before meals. If the patient cannot swallow the capsule whole, you can dissolve its contents in a small amount of water or fruit juice (do not dissolve in carbonated drinks). The resulting solution of the drug should be drunk immediately after cooking, with an additional 1/2 cup of water.

Symptoms of gastroesophageal reflux, such as heartburn, acid belching.

The usual dose of Gastrozol® is 10 mg (1 capsule) once a day.

The maximum daily dose of the drug should not exceed 20 mg. The lowest effective dose should always be used. The maximum course of treatment without consulting a doctor is 14 days. The interval between 14-day courses of treatment should be at least 4 months.

If there is no relief of symptoms within 2 weeks or they worsen, you should consult your doctor!

Use of the drug in special cases

The possibility of using the drug Gastrozol® in special cases is evaluated by the doctor.

Impaired renal function.

No dose adjustment is required.

Impaired liver function.

In patients with impaired liver function, the bioavailability and clearance of omeprazole increases. Please consult your doctor before use.

Advanced age.

Despite the fact that the metabolic rate of omeprazole decreases in the elderly, dose adjustment is not required when using the drug in a daily dose of 20 mg or less.

Overdose

Symptoms: dizziness, confusion, apathy, depression, drowsiness, headache, visual disturbances, vascular dilatation, tachycardia, nausea, vomiting, flatulence, abdominal pain, diarrhea, increased sweating, “dry” mouth.

Treatment: symptomatic. If necessary, gastric lavage, the appointment of activated charcoal. Hemodialysis is not effective enough.

Special instructions

Omeprazole is not intended for use in case of accidental heartburn (heartburn less than 2 times a week).

Before starting therapy with omeprazole, it is necessary to exclude the presence of a malignant process in the upper gastrointestinal tract, since taking omeprazole can mask the symptoms and delay the correct diagnosis.

A decrease in the secretion of hydrochloric acid in the stomach under the action of proton pump inhibitors leads to an increase in the growth of normal intestinal microflora and may lead to a slight increase in the risk of intestinal infections caused by Salmonella spp., Campylobacter spp., and Clostridium difficile bacteria.

A decrease in hydrochloric acid secretion can lead to an increase in the concentration of chromogranin A (CgA), which affects the results of examinations for the detection of neuroendocrine tumors, so to prevent this effect, it is necessary to temporarily stop taking omeprazole 5 days before the CgA concentration study. If the CgA concentration has not returned to normal during this time, the study should be repeated.

The risk-benefit ratio of long-term (more than 1 year) maintenance therapy with omeprazole should be regularly evaluated. There is evidence of an increased risk of vertebral, wrist, and femoral head fractures, mainly in elderly patients or in the presence of other risk factors. Patients at risk of developing osteoporosis should be given adequate intake of vitamin D and calcium.

Patients treated with omeprazole for at least three months have been reported to have severe hypomagnesaemia, with symptoms such as fatigue, delirium, seizures, dizziness, and ventricular arrhythmia. In most patients, hypomagnesemia was stopped after the withdrawal of proton pump inhibitors and the introduction of magnesium preparations.

Patients receiving omeprazole therapy for a long time, especially in combination with digoxin or other drugs that reduce the content of magnesium in blood plasma (diuretics), need regular monitoring of magnesium content.

Omeprazole, like all drugs that reduce acidity, can lead to a decrease in the absorption of vitamin_B12 (cyanocobalamin). This should be kept in mind for patients with a reduced supply of vitamin_B12 during long-term therapy.

Glandular cysts in the stomach were more frequently observed in patients taking oral medications that lower the secretion of gastric glands for a long time. These phenomena are caused by physiological changes as a result of inhibition of hydrochloric acid secretion, and are subject to reverse development against the background of continuing therapy.

Influence on the ability to drive vehicles and mechanisms

During treatment with omeprazole, dizziness, confusion, drowsiness, visual impairment may occur, so caution should be exercised when driving vehicles or operating other mechanisms and performing other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Storage conditions

Store at a temperature not exceeding 25 ° C.

Keep out of reach of children.

Shelf

life is 2 years.

Active ingredient

Omeprazole

Dosage form

Capsules