Zolser

Zolser has antiulcer activity.

Indications Zolcera

It is used for the following disorders:

• ulcerative lesions affecting the gastrointestinal tract (also to prevent relapses);
• reflux esophagitis;
• conditions with increased secretory activity (stress-related ulcers in the gastrointestinal tract, gastrinoma, polyendocrine adenomatosis and general mastocytosis);
• NSAID-associated gastropathy.

Destruction of Helicobacter pylori in infected people with gastrointestinal ulcers (as an integral part of complex treatment).

Release form

The substance is released in enteric-coated capsules with a volume of 20 mg. There are 10 capsules in a blister pack; there are 10 packs in a box.

Pharmacodynamics

The drug is a hydrogen pump blocker, reduces acid production by slowing down the action of H ⁺ /K ⁺ -ATPase inside the parietal gastric glandulocytes, which prevents the final phase of HCl excretion. Zolser is a prodrug that becomes active in the acidic environment of the excretory canals of the parietal glandulocytes. Without reference to the origin of the irritant, it reduces stimulated and basal excretion.

The anti-excretion effect after taking 20 mg of the substance develops over 60 minutes, reaching a peak after 120 minutes. Slowing down 50% of maximum excretory processes lasts 24 hours.

A single dose per day leads to effective and rapid suppression of the secretory function of the stomach (day and night). The maximum effect develops after 4 days, and disappears by the end of the 3-4th day from the moment of completion of drug use.

In people with ulcers in the duodenum, maintenance of the intragastric pH at 3 after administration of 20 mg of the drug lasts for 17 hours.

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Pharmacokinetics

Absorption of the drug from the small intestine is complete. The overall bioavailability values of the drug after the first dose are 35%, and with repeated use they increase to almost 60%. Food intake does not affect the level of bioavailability of the drug. The severity of suppression of excretion processes is determined by AUC values.

Intraplasmic protein synthesis is approximately 95%.

Almost all of the drug undergoes intrahepatic metabolic processes. Metabolic products (sulfide with sulfone, as well as hydroxyomeprazole) do not have a significant effect on the secretion of hydrochloric acid.

About 80% of metabolic products are excreted in urine, and the remainder in feces. The half-life is on average about 40 minutes. This indicator does not change in case of repeated administration of Zolsera.

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Dosing and administration

The capsules are taken orally, often in the morning, without chewing, with plain water (this occurs immediately before eating or during a meal).

In case of exacerbation of reflux esophagitis, ulcers or gastropathy associated with the administration of NSAIDs, it is necessary to take 20 mg of the drug once a day. For people with a severe stage of reflux esophagitis, the dose is increased to 40 mg of the substance with a single dose per day.

Therapy for intestinal ulcers lasts for 2-3 weeks (if necessary, extended to 4-5 weeks). For esophagitis or gastric ulcers, a 1-2 month course is required.

People who are resistant to other antiulcer medications are required to take 40 mg of the drug per day. The treatment cycle for intestinal ulcers lasts 1 month; for gastric ulcers or reflux esophagitis, 2 months of therapy are required.

For gastrinoma, 60 mg of the drug is used. If necessary, the dose is increased to 80-120 mg per day (under such circumstances, the dosage is divided into 2-3 uses).

To prevent recurrence of ulcer development, 10 mg of the drug is used once a day.

When destroying Helicobacter pylori, the following schemes are used:

• "Triple" treatment - a 7-day course, in which 20 mg of omeprazole, 1000 mg of amoxicillin and 0.5 g of clarithromycin are used twice a day. 20 mg of omeprazole, 0.4 g of metronidazole and 0.25 g of clarithromycin can also be used (also twice a day). Another regimen is a single dose of 40 mg of omeprazole, as well as a three-time dose of 0.5 g of amoxicillin and 0.4 g of metronidazole;
• "double" treatment - a 14-day course, during which 20-40 mg of omeprazole and 0.75 g of amoxicillin are used, 2 times a day. A cycle can be carried out with a single administration of 40 mg of omeprazole and 3 times a day of 0.5 g of clarithromycin (or 750-1500 mg of amoxicillin 2 times a day).

People with liver failure need to take 10-20 mg of the drug.

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Use Zolcera during pregnancy

The drug should not be used during lactation or pregnancy. If a lactating woman needs to take the drug, she should stop breastfeeding.

Contraindications

Contraindicated for use in people with ulcerative degeneration of a malignant nature.

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Side effects Zolcera

The introduction of capsules may provoke the development of certain side effects:

• digestive disorders: nausea, diarrhea or constipation, abdominal pain, bloating and vomiting. Rarely, liver enzyme levels increase or taste disorders develop. Stomatitis or dry mouth may occur. In people with previous liver diseases, hepatitis (sometimes accompanied by jaundice) or liver dysfunction may occur;
• problems affecting the hematopoietic system: thrombocyto-, pancyto- or leukopenia, as well as agranulocytosis, may occur;
• disorders associated with the functioning of the nervous system: people with existing somatic pathologies of a severe nature experience headaches, depression, agitation and dizziness. People with a history of severe liver disease develop encephalopathy;
• pathologies in the musculoskeletal system: myasthenia, arthralgia or myalgia may occur;
• lesions of the epidermal layer: occasionally itching or rashes appear. MEE, photosensitivity or alopecia may also develop;
• signs of allergy: Quincke's edema, anaphylaxis, urticaria, as well as bronchial spasm, fever and tubulointerstitial nephritis;
• other disorders: malaise, hyperhidrosis, gynecomastia, visual disturbances, peripheral edema are occasionally observed. In addition, with long-term treatment, glandular cysts form inside the stomach (due to the slowing down of the HCl secretion processes; this disorder is curable and has a benign nature).

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Overdose

Symptoms of intoxication include blurred vision, nausea, confusion or drowsiness, as well as headaches, arrhythmia, severe dryness affecting the oral mucosa, and tachycardia.

Symptomatic measures are taken. Hemodialysis does not have sufficient effect.

Interactions with other drugs

The drug can significantly reduce the absorption of ampicillin esters, ketoconazole with itraconazole and iron salts (omeprazole leads to an increase in gastric pH).

Because the drug slows down the activity of hemoprotein P450, it can increase the values of indirect anticoagulants, diazepam and phenytoin (substances whose liver metabolic processes occur with the participation of hemoprotein CYP2C19) and weaken their excretion. In such cases, it may sometimes be necessary to reduce the doses of these medications.

At the same time, long-term administration of 20 mg omeprazole once a day together with theophylline or naproxen, and together with caffeine, metoprolol or piroxicam, propranolol or diclofenac, cyclosporine, ethyl alcohol, as well as estradiol with quinidine or lidocaine does not cause changes in their plasma parameters.

Zolser potentiates the retarding effect of other medications on hematopoietic function.

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Storage conditions

Zolser should be stored in a dark and dry place, out of the reach of small children. Temperature – standard.

Shelf life

Zolser can be used within a 24-month period from the date of manufacture of the therapeutic substance.

Application for children

In pediatrics, Zolser is not prescribed (except in cases of vital necessity).

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Analogues

Analogues of the drug are Losek, Ortanol with Omez and Ultop with Omeprazole.

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