Gastrozole, 10 mg capsules 28 pcs

Pharmacotherapeutic group: gastric gland secretion reducing agent – proton pump inhibitor

ATX code: A02BC01

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 effects of omeprazole occur within the first hour and last for 24 hours. Maximum effect is reached after 2 hours. After discontinuation of the drug secretory activity is fully restored in 3 to 5 days.

Pharmacokinetics

Intake

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

Distribution

The binding to plasma proteins is about 95%.

Metabolism

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

The elimination half-life (T1/2) is 0 5 – 1 hour. It is excreted as metabolites by kidneys (70 – 80%) and in the bile (20 – 30%).

Pharmacokinetics in special clinical cases

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

Indications

Active ingredient

Composition

Omeprazole pellets – 117.5 mg, containing:

the active substance: omeprazole – 10.0 mg;

excipients: Mannitol – 19.97 mg, sucrose – 32.11 mg, disodium hydrophosphate – 1.49 mg, sodium lauryl sulfate – 0.40 mg, lactose monohydrate – 4.00 mg, calcium carbonate – 4.00 mg, hypromellose (hydroxypropyl methylcellulose E-5) – 10.28 mg, methacrylic acid and ethyl acrylate copolymer [1:1](L-30D) – 29.37 mg, propylene glycol – 0.95 mg, diethyl phthalate – 2.94 mg, cetyl alcohol – 0.88 mg, sodium hydroxide – 0.18 mg, polysorbate-80 – 0.35 mg, povidone (polyvinylpyrrolidone, povidon K-30) – 0.30 mg, titanium dioxide – 0.21 mg, talc – 0.07 mg.

The composition of the hard gelatin capsule shell:

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

Cup: titanium dioxide (E171) – 1.3333%, sunset yellow dye (E 110) – 0.0044%, quinoline yellow (E 104) – 0.9197%, gelatin – up to 100%.
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How to take, the dosage

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

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

The usual dose of Gastrozole® is 10 mg (1 capsule) once daily.

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 a physician’s consultation is 14 days. The interval between 14-day courses of treatment should be at least 4 months.

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

The use of the drug in special cases

The possibility of using Gastrozole® in special cases is assessed by a physician.

Disordered renal function.

Dose adjustment is not required.

Liver function impairment.

The bioavailability and clearance of omeprazole are increased in patients with hepatic impairment. A physician should be consulted before use.

Elderly age.

Although the metabolic rate of omeprazole is decreased in elderly patients, no dose adjustment is required when using the drug at a daily dose of 20 mg or less.

Interaction

You should consult your doctor before taking Gastrozole® if you are receiving treatment with one or more of the drugs mentioned in this section.

The decrease in gastric hydrochloric acid secretion during treatment with omeprazole and other proton pump inhibitors may lead to decreased or increased absorption of other drugs whose absorption depends on the acidity of the environment.

Like other drugs that reduce gastric acidity, treatment with omeprazole may lead to decreased absorption of ketoconazole, itraconazole, posaconazole, erlotinib, iron drugs and cyanocobalamin. Their co-administration with omeprazole should be avoided.

The bioavailability of digoxin when coadministered with omeprazole is increased by 10% (dosing regimen of digoxin may need to be adjusted). Caution should be exercised when concomitant use of 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. Increased pH on omeprazole therapy may affect the absorption of antiretroviral drugs.

An interaction at the level of CYP2C19 isoenzyme is also possible. When omeprazole and some antiretroviral drugs such as atazanavir and nelfinavir are used together, a decrease in their serum concentrations is noted during therapy with omeprazole.

The concomitant use of atazanavir with omeprazole decreases the area under the “concentration-time” curve by 75%. In this regard, co-administration of omeprazole with antiretroviral drugs such as atazanavir and nelfinavir is contraindicated.

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

In concomitant use of omeprazole with clopidogrel a decrease in the antiaggregant effect of the latter has been observed.

Special Instructions

Omeprazole is not indicated for occasional heartburn (heartburn less than 2 times a week).

Before starting therapy with omeprazole, the presence of a malignant process in the upper gastrointestinal tract should be excluded, as taking omeprazole may mask symptoms and delay a correct diagnosis.

The reduction of gastric hydrochloric acid secretion by proton pump inhibitors leads to increased growth of normal gut microflora and may lead to a slightly increased risk of intestinal infections caused by Salmonella spp., Campylobacter spp. and Clostridium difficile bacteria.

The decrease in hydrochloric acid secretion may increase chromogranin A (CgA) concentrations, which influences neuroendocrine tumor screenings; therefore, to prevent this effect, omeprazole should be temporarily stopped 5 days before testing CgA concentrations. If CgA concentrations have not returned to normal during this time, the study should be repeated.

The risk-benefit ratio of long-term (>1 year) omeprazole maintenance therapy should be evaluated regularly. There is evidence of an increased risk of vertebral, carpal, and femoral head fractures, primarily in elderly patients or in the presence of other risk factors. Patients at risk for osteoporosis should have adequate vitamin D and calcium intake.

Severe hypomagnesemia has been reported in patients treated with omeprazole for at least three months, with symptoms such as fatigue, delirium, seizures, dizziness, and ventricular arrhythmias. In most patients, hypomagnesemia resolved after discontinuation of proton pump inhibitors and administration of magnesium preparations.

Patients on long-term therapy with omeprazole, especially in combination with digoxin or other magnesium-lowering drugs (diuretics), require regular monitoring of magnesium.

Omeprazole, like all acid-lowering drugs, may decrease absorption of vitamin B12(cyanocobalamin). This should be kept in mind in patients with reduced vitamin B12 supply during long-term therapy.

The formation of glandular cysts in the stomach has been observed more frequently in patients taking oral medications that decrease gastric gland secretion over a long period of time. These phenomena are due to physiologic changes resulting from inhibition of hydrochloric acid secretion, and are reversed with continuation of therapy.

Influence on driving, operating machinery

Contraindications

Hypersensitivity to omeprazole, substituted benzimidazoles or other drug components.

Simultaneous use with nelfinavir, atazanavir, erlotinib, posaconazole.

Above 18 years of age.

Precautions for use

Consult a physician before using the drug in the following cases:

– in the presence of previously diagnosed peptic ulcer disease; severe liver disease accompanied by liver failure; jaundice; previous gastrointestinal surgery;

– in the presence of “alarming” symptoms: significant spontaneous weight loss, recurrent vomiting, vomiting with blood admixture, changes in stool color (tarry stools – melena), impaired swallowing;

– if new symptoms appear or existing symptoms change from the gastrointestinal tract;

– In the presence of osteoporosis;

– In the presence of ongoing symptomatic treatment for digestive distress or persistent heartburn (for 4 weeks or more);

– When used concomitantly with one or more of the following drugs clopidogrel, digoxin, erlotinib, ketoconazole, itraconazole, warfarin, cilostazol, diazepam, phenytoin, saquinavir, tacrolimus, clarithromycin, voriconazole, rifampicin, St. John’s wort preparations (see See section Interaction with other medicinal products).

Side effects

The frequency of side effects is stated according to the following gradation: very frequently (≥1/10); frequently (≥1/100, < 1/10); infrequently (≥1/1000, < 1/100); rarely (≥1/10000, < 1/1000); very rarely (< 1/10000).

Allergic reactions: infrequent – urticaria, skin rash, itching; rare – fever, urticaria, angioedema, anaphylactoid reactions; very rare – eosinophilia.

Gastrointestinal tract disorders: frequent – nausea, vomiting, abdominal pain, diarrhea or constipation, flatulence; infrequent – increased activity of “liver” enzymes (transaminases) and alkaline phosphatase (reversible nature), perversion of taste (usually passes after discontinuation of therapy); rarely – dry mouth, stomatitis, gastrointestinal candidiasis, hepatitis (with or without jaundice), microscopic colitis, tongue discoloration to brownish black, and appearance of benign salivary gland cysts when concomitantly used with clarithromycin (phenomena are reversible after discontinuation of therapy); very rarely – liver failure (in patients with previous severe liver disease).

Nervous system disorders: frequently – headache; infrequently – dizziness, paresthesia, somnolence, insomnia; rarely – agitation, reversible confusion, depression; very rarely – aggression, confusion, hallucinations; with severe liver disease – encephalopathy.

Skin and subcutaneous tissue disorders: infrequent – dermatitis; rare – photosensitization (reddening of the skin), alopecia; very rare – erythema multiforme exudative, Stevens-Johnson syndrome (severe erythema multiforme, characterized by the appearance of spots and blisters on the skin and mucous membranes against high temperature and joint pain), toxic epidermal necrolysis; incidence unknown – subacute cutaneous lupus erythema.

Visual organ disorders: infrequent – visual disturbances, including decrease of visual fields, decrease of visual acuity and clarity of visual perception (usually relieved after discontinuation of therapy).

Hearing organ and labyrinth disorders: infrequent – disorders of auditory perception, including “ringing in the ears” (usually subsides after discontinuation of therapy), vertigo.

Skeletal, musculoskeletal and connective tissue disorders: infrequent fractures of the vertebrae, carpal bones, femoral head (see section “Special directions”); rarely – myalgia (muscle pain), arthralgia (joint pain), muscle weakness.

Respiratory system disorders: rarely – bronchospasm.

Renal and urinary tract: rarely – interstitial nephritis.

Hematopoietic organs: rare – leukopenia, thrombocytopenia; very rare – agranulocytosis, pancytopenia.

Endocrine system: very rare – gynecomastia.

Others: infrequent – peripheral edema, malaise; rare – increased sweating, hyponatremia; very rare – hypomagnesemia, hypocalcemia due to severe hypomagnesemia.

There have been reported cases of glandular cysts in the stomach in patients who have taken drugs that decrease gastric gland secretion for a long period of time; the cysts are benign and resolve on their own with continuation of therapy.

Overdose

Symptoms: dizziness, confusion, apathy, depression, somnolence, headache, visual disturbances, dilated blood vessels, tachycardia, nausea, vomiting, flatulence, abdominal pain diarrhea, increased sweating, “dry” mouth.

Pregnancy use

The results of three prospective epidemiological studies (more than 1000 observations) have shown that the use of omeprazole in pregnant women has no adverse effect on pregnancy and fetal/newborn health. However, it is recommended that a physician be consulted before using the drug during pregnancy.

Similarities