Gastrozol - description of the drug, instructions for use, reviews

Release form and composition

Dosage form - capsules: size No. 2, hard gelatin, opaque, body - light pink, cap - pinkish-brown; contents – pellets of white or almost white color (7 or 10 pcs. in contour-free packaging, 1 or 2 packs in a cardboard pack; 10, 14 or 28 pcs. in polymer cans, 1 can in a cardboard pack).

Active ingredient: omeprazole, 1 capsule – 20 mg.

Additional components: calcium carbonate, sodium hydrogen phosphate (disodium phosphate disubstituted), lactose, sodium lauryl sulfate, hypromellose (hydroxypropyl methylcellulose), sucrose, methacrylic acid and ethyl acrylate copolymer (methacrylic acid copolymer L30D), cetyl alcohol, diethyl phthalate, sodium hydroxide, propylene glycol, polysorbate 80 (Tween-80), titanium dioxide, povidone (polyvinylpyrrolidone), talc, mannitol.

Capsule composition (body and cap): gelatin, methyl parahydroxybenzoate (methylhydroxybenzoate), titanium dioxide (E171), propyl parahydroxybenzoate (propylhydroxybenzoate), red iron oxide (E172); or gelatin, titanium dioxide (E171) and iron oxide red (E172).

pharmachologic effect

Pharmacodynamics

Gastrozole is a proton pump inhibitor and reduces the production of gastric acid by inhibiting the activity of H+/K+-ATPase in the parietal cells of the stomach, resulting in the blocking of the final stage of hydrochloric acid. The drug is a prodrug and is activated in an acidic environment characteristic of the secretory tubules of parietal cells.

Omeprazole reduces stimulated and basal secretion, regardless of the type of stimulus. After taking 20 mg of Gastrozol, the antisecretory effect appears within the first hour (maximum after 2 hours). Maximum secretion is inhibited by 50% within 24 hours. A single daily dose of the drug guarantees rapid and effective suppression of daytime and nighttime secretion of the gastric glands, which reaches a maximum after 4 days of treatment and disappears 3-4 days after completion of the course of therapy. In patients with duodenal ulcer, taking 20 mg of Gastrozol stabilizes the intragastric acidity (pH) at 3.0 for 17 hours.

Pharmacokinetics

The drug has a high degree of absorption, and its maximum concentration in the body is observed 0.5–3.5 hours after oral administration. Bioavailability is 30–40%, increasing to almost 100% in case of liver failure. The active component of the drug has increased lipophilicity and easily penetrates the parietal cells of the stomach, binding to plasma proteins (albumin and acid α1-glycoprotein) by 90–95%.

The half-life of omeprazole is 0.5–1 hour (with hepatic dysfunction – 3 hours), and clearance reaches 500–600 ml/min. The active substance Gastrozol is almost completely metabolized in the liver under the influence of the CYP2C19 enzyme system, forming 6 pharmacologically inactive metabolites (hydroxyomeprazole, sulfonic and sulfide derivatives, etc.). The drug belongs to the group of inhibitors of the CYP2C19 isoenzyme and is excreted through the kidneys (70–80%) and bile (20–30%). Chronic renal failure reduces excretion in proportion to the decrease in creatinine clearance. In elderly patients, the bioavailability of omeprazole increases, and the rate of its elimination decreases.

Comparison of addiction between Gastrozole and Omeprazole

Like safety, addiction also involves many factors that must be considered when evaluating a drug.

So, the totality of the values ​​of such parameters as “o syndrome” for Gastrozole is quite similar to the similar values ​​for Omeprazole. Withdrawal syndrome is a pathological condition that occurs after the cessation of intake of addictive or dependent substances into the body. And resistance is understood as initial immunity to a drug; in this it differs from addiction, when immunity to a drug develops over a certain period of time. The presence of resistance can only be stated if an attempt has been made to increase the dose of the drug to the maximum possible. At the same time, Gastrozole has a fairly low “syndrome” value, just like Omeprazole.

Indications for use

• Exacerbation of peptic ulcer of the stomach and duodenum;
• Reflux esophagitis;
• Gastropathy induced by the use of nonsteroidal anti-inflammatory drugs (NSAID gastropathy);
• Hypersecretory conditions (polyendocrine adenomatosis, stress ulcers of the gastrointestinal tract, systemic mastocytosis, Zollinger-Ellison syndrome);
• Helicobacter pylori infection in patients with gastric and duodenal ulcers (as part of complex therapy).

The drug is also used to prevent gastric and duodenal ulcers.

Application in medical practice

Omeprazole can be used to treat gastroesophageal reflux disease (GERD), peptic ulcers, erosive esophagitis, Zollinger-Ellison syndrome and eosinophilic esophagitis[4][5].

Peptic ulcers

Peptic ulcers can be treated with omeprazole. Treatment of Helicobacter pylori infection can be completed by taking triple therapy with a combination of omeprazole, amoxicillin and clarithromycin for 7-14 days[6]. Amoxicillin can be replaced by metronidazole for patients allergic to penicillin[7].

Treatment of reflux in children

Little evidence was found that medications work in children under one year of age, especially for functional reflux; Mixed evidence has been found as to whether Gaviscon Infant® helps, and that in children with reflux disease (changes on pH testing or on endoscopy) medications such as omeprazole and lansoprazole are likely to help. In older children, proton pump inhibitors and histamine antagonists work better in terms of improvement in symptoms, endoscopic findings, and pH measurements, but no meta-analysis has been performed or whether one drug is superior to the other [8][9].

Instructions for use of Gastrozol: method and dosage

The drug is taken orally by swallowing the capsules whole with a small amount of water, usually in the morning, immediately before meals or during meals.

Recommended doses depending on indications:

• Exacerbation of duodenal ulcer: 1 capsule per day for 2-4 weeks, if necessary, increase the dose to 2 capsules;
• Exacerbation of duodenal ulcer and erosive-ulcerative esophagitis: 1-2 capsules per day for 4-8 weeks;
• NSAID gastropathy: 1 capsule per day for 4-8 weeks;
• Helicobacter pylori infection: 1 capsule 2 times a day in combination with antibacterial agents, course – 7 days;
• Zollinger-Ellison syndrome: the dose is set individually depending on the initial level of gastric secretion. The initial dose is usually 3 capsules per day, if necessary, it is increased to 4-6 capsules and the dose is divided into 2 doses;
• Prevention of relapses of gastric and duodenal ulcers: 1 capsule per day;
• Prevention of relapses of reflux esophagitis: 1 capsule per day for a long time (up to 6 months).

Notes

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   Minardi, Maria Eugenia; Zagari, Rocco Maurizo; Grilli, Diego; Magrini, Nicola; Bazzoli, Franco. Meta-analysis: Duration of First-Line Proton-Pump Inhibitor–Based Triple Therapy for
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Side effects

• Digestive system: diarrhea/constipation, flatulence, nausea, vomiting, abdominal pain; rarely - taste disturbances, increased activity of liver transaminases, formation of gastric glandular cysts during long-term treatment (they are reversible and benign); in some cases – stomatitis, dry mouth; in patients with previous severe liver disease - impaired liver function, hepatitis (including jaundice);
• Musculoskeletal system: in some cases – myasthenia gravis, arthralgia, myalgia;
• Central and peripheral nervous system: in patients with concomitant severe somatic diseases - agitation, headache, depression, dizziness; in patients with previous severe liver diseases - encephalopathy;
• Hematopoietic system: in some cases - agranulocytosis, thrombocytopenia, pancytopenia, leukopenia;
• Dermatological reactions: rarely - rash and/or itching of the skin; in some cases - alopecia, photosensitivity, exudative erythema multiforme;
• Allergic reactions: fever, urticaria, bronchospasm, angioedema, anaphylactic shock, interstitial nephritis;
• Other: blurred vision, malaise, peripheral edema, gynecomastia, increased sweating.

Content

• 1 Application in medical practice 1.1 Peptic ulcers
• 1.2 Treatment of reflux in children

Overdose

A single oral dose of Gastrozol in doses not exceeding 400 mg (2 capsules) did not lead to any severe symptoms. A single dose of omeprazole 560 mg in adult patients was accompanied by signs of moderate intoxication. Increasing the dose did not change the rate of drug elimination and did not require specific treatment.

Symptoms of overdose are: nausea, vomiting, flatulence, diarrhea, headache, dizziness, clouded consciousness, apathy, vascular dilatation, tachycardia. In this case, symptomatic treatment and administration of activated carbon are prescribed, and, if necessary, the stomach is washed.

special instructions

Before prescribing Gastrozol, it is necessary to examine the patient to exclude the presence of a malignant process, especially with gastric ulcer, since omeprazole can mask symptoms and thereby delay the timely making of the correct diagnosis.

Eating does not affect the effectiveness of the drug.

Impact on the ability to drive vehicles and complex mechanisms

Since treatment may be accompanied by side effects such as drowsiness, dizziness and blurred vision, caution must be exercised when driving or operating complex machinery that requires increased concentration and immediate psychomotor reactions.

Drug interactions

Omeprazole increases the pH of the stomach, so it can reduce the absorption of ketoconazole, itraconazole, iron salts and ampicillin esters.

Omeprazole is an inhibitor of cytochrome P450 isoenzymes, and therefore may increase plasma concentrations and reduce the excretion of drugs metabolized in the liver with the participation of CYP2C19 (for example, phenytoin), indirect anticoagulants and diazepam. For this reason, it may be necessary to reduce the dosage of these medicines.

According to the instructions, Gastrozol enhances the inhibitory effect of other drugs on the hematopoietic system.

Storage

This medicine should be stored at room temperature not exceeding 25 degrees .

In addition, pets and small children should not have access to the place where Gastrozol was placed. The drug can be stored for 3 years, after which it must be disposed of.

Reviews of Gastrozole

According to reviews, Gastrozol is a fairly effective treatment for all conditions indicated in its indications for use. However, some patients complain of side effects while taking the drug, such as headache, nausea, abdominal pain and allergic reactions. But it is worth considering that all these symptoms are often mild or disappear on their own in the next stages of therapy. Patients also note the rather high cost of Gastrozole compared to its analogues, which also contain omeprazole.

Comparison of the safety of Gastrozole and Omeprazole

The safety of a drug includes many factors.

At the same time, with Gastrozole it is quite similar to Omeprazole. It is important where the drug is metabolized: drugs are excreted from the body either unchanged or in the form of products of their biochemical transformations. Metabolism occurs spontaneously, but most often involves major organs such as the liver, kidneys, lungs, skin, brain and others. When assessing the metabolism of Gastrozole, as well as Omeprazole, we look at which organ is the metabolizing organ and how critical the effect on it is.

The risk-benefit ratio is when the prescription of a drug is undesirable, but justified under certain conditions and circumstances, with the obligatory observance of caution in use. At the same time, Gastrozole does not have any risks when used, just like Omeprazole.

Also, when calculating safety, it is taken into account whether only allergic reactions occur or possible dysfunction of the main organs. In other matters, as well as the reversibility of the consequences of the use of Gastrozole and Omeprazole.