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Composition:


active ingredient: pantoprazole;


1 gastro resistant tablet contains pantoprazole sodium sesquihydrate equivalent to pantoprazole 20 mg;


excipients: mannitol (E 421), crospovidone, sodium carbonate anhydrous, hydroxypropylcellulose, calcium stearate, hypromellose, iron oxide yellow (E 172), methacrylate copolymer dispersion, triethylcitrate.


Dosage form. Gastro-resistant tablets.


Basic physical and chemical properties: tablets of 20 mg: light yellow color, coated with an enteric coating, Oval biconvex tablets, smooth on both sides.


Pharmacotherapeutic group. A drug for the treatment of acid-dependent diseases. Proton pump inhibitors. ATX code A02B C02.


Pharmacological properties.


Pharmacodynamics.


Mechanism of action. Pantoprazole is a substituted benzimidazole that inhibits the secretion of hydrochloric acid in the stomach by specifically blocking the proton pumps of parietal cells. Pantoprazole is transformed into the active form in an acidic environment in parietal cells, where it inhibits the enzyme H+-K+-ATPase, that is, it blocks the final stage of hydrochloric acid production in the stomach. Inhibition is dose-dependent and affects both basal and stimulated acid secretion. Most patients are relieved of symptoms Within 2 weeks. The use of pantoprazole, as well as other proton pump inhibitors (PPIs) and H2 receptor inhibitors, reduces stomach acidity and thus increases gastrin secretion in proportion to the decrease in acidity. The increase in gastrin secretion is reversible. Since pantoprazole binds the enzyme distally to the cellular receptor, it can inhibit hydrochloric acid secretion independently of stimulation with other substances (acetylcholine, histamine, gastrin). The effect of oral and intravenous administration of the drug is the same.


When using pantoprazole, the level of gastrin increases on an empty stomach. With short-term use, in most cases it does not exceed the upper limit of the norm. With long-term treatment, the level of gastrin in most cases doubles. Its excessive increase occurs only in isolated cases. As a result, a small number of patients with long-term treatment have a weak or moderate increase in specific endocrine (ECL) cells in the stomach (similar to adenomatoid hyperplasia). However, according to The conducted studies, the formation of progenitor cells of neuroendocrine tumors (atypical hyperplasia) or neuroendocrine stomach tumors, which were found in animal studies, was not observed in humans.


Based on the results of animal studies, the effect of long-term (more than one year) treatment with pantoprazole on the Endocrine parameters of the thyroid gland cannot be completely excluded.


During treatment with antisecretory drugs, the level of gastrin in the blood serum increases in response to a decrease in acid secretion. In addition, due to a decrease in stomach acidity, the level of chromogranin a (CgA) increases. Elevated CgA levels may affect research results in the diagnosis of neuroendocrine tumors. Available published data suggest that PPI treatment should be discontinued within 5 days to 2 weeks prior to CGA measurements. This allows CgA levels to return to the normal range, which may be falsely elevated after PPI treatment.


Pharmacokinetics.


Suction. Pantoprazole is rapidly absorbed, and the maximum concentration in blood plasma (Cmax) is reached after a single oral dose of 20 mg. On average,2-2.5 hours after administration, Cmax is reached at a level of about 1-1. 5 mcg/ml; the concentration does not change after repeated administration of the drug. Pharmacokinetic properties do not change after a single or repeated dose. In the dose range from 10 to 80 mg, the plasma pharmacokinetics of pantoprazole remain linear with both oral and intravenous administration. It was found that the absolute bioavailability of tablets is about 77 %. Simultaneous food intake does not affect AUC (area under the concentration-time curve) or Cmax, and, accordingly, bioavailability. With simultaneous food intake, only the variability of the latent period increases.


Distribution. The Binding of pantoprazole to Serum Proteins is about 98 %. The volume of distribution is about 0.15 l/kg.


Biotransformation. The substance is metabolized almost exclusively in the liver. The main metabolic pathway is demethylation by CYP2C19 followed by sulfate conjugation; other metabolic pathways include oxidation by CYP3A4. Output. The final half – life (T1/2) is about 1 hour, and the clearance is 0.1 L/H/kg. There were several cases of delayed withdrawal. Due to the specific binding of pantoprazole to proton pumps of parietal cells, T1/2 does not correspond to a much longer duration of action (inhibition of acid secretion).


The main part of pantoprazole metabolites is excreted in the urine (about 80 %), the rest is excreted in the faeces. The main metabolite in both serum and urine is desmethylpantoprazole conjugated with sulfate. T1/2 of the main metabolite (about 1.5 hours) is not much higher than T1 / 2 of pantoprazole.


Special groups of patients.


Slow metabolizers.


About 3% of Europeans have low functional activity of the enzyme CYP2C19; such people are called slow metabolizers. In the organisms of such individuals, the metabolism of pantoprazole is probably mainly catalyzed by the enzyme CYP3A4. After taking a single dose of 40 mg pantoprazole, the average AUC was approximately 6 times higher in slow metabolizers than in individuals with the functionally active enzyme CYP2C19 (fast metabolizers). The average Cmax increased by about 60 %. These results do not affect the dosage of pantoprazole.


Patients with renal insufficiency.


There are no recommendations for reducing the dose of pantoprazole in patients with reduced renal function, including those on dialysis. As in healthy people, the T1/2 of pantoprazole in them is short. Only very small amounts of pantoprazole are dialyzed. Despite the fact that the main metabolite has a moderately long T1/2 (2-3 hours), elimination is rapid, so accumulation does not occur.


Patients with hepatic insufficiency.


Although in patients with cirrhosis of the liver (Classes A and B on the Child‒Pugh scale), T1/2 increases to 3-6 hours, and AUC increases 3-5 times, Cmax increases only slightly – 1.3 times compared to that in healthy volunteers.


Elderly patients.


A small increase in AUC and Cmax in older volunteers compared to younger volunteers is also not clinically significant.


Children.


After a single oral dose of 20 or 40 mg of pantoprazole, the AUC and Cmax in children aged 5 to 16 years were within the corresponding values in adults. After a single intravenous administration of pantoprazole at doses of 0.8 or 1.6 mg/kg to children aged 2 to 16 years, there was no significant association between pantoprazole clearance and age or body weight. AUC and volume of distribution were consistent with data obtained in adult studies.


Clinical characteristics.


Indications.


Adults and children over 12 years of age.


- Symptomatic treatment of gastroesophageal reflux disease.


- Long-term treatment and Prevention of relapses of reflux esophagitis.


Adults.


- Prevention of gastric and duodenal ulcers caused by taking non-selective nonsteroidal anti-inflammatory drugs (NSAIDs) in patients at risk who should use NSAIDs for a long time.


Contraindications.


Hypersensitivity to the active substance, benzimidazole derivatives or to any other component of the drug.


Interactions with other drugs and other types of interactions.


Medicinal products whose absorption depends on PH.


Due to complete and prolonged inhibition of hydrochloric acid secretion, pantoprazole may reduce the absorption of drugs whose bioavailability depends on the pH of gastric juice (for example, some antifungal drugs, such as ketoconazole, itraconazole, posaconazole, or other drugs, such as erlotinib).


HIV protease inhibitors.

Concomitant use of pantoprazole with HIV protease inhibitors (such as atazanavir), whose absorption depends on intragastric ph, is not recommended due to a significant decrease in their bioavailability (see the section "special applications").


If the combined use of HIV protease inhibitors with PPIs cannot be avoided, careful clinical monitoring (for example, viral load) is recommended. Do not exceed the daily dose of pantoprazole 20 mg. It may be necessary to adjust the dose of HIV protease inhibitors.


Coumarin anticoagulants (fenprocumone and warfarin).


Co-administration of pantoprazole with warfarin or fenprocumone did not affect the pharmacokinetics of warfarin, fenprocumone, or INR (international normalized index). However, an increase in INR and an increase in prothrombin time were recorded in patients who co-administered PPIs and warfarin or fenprocumone. An increase in INR and an extension of prothrombin time can lead to the development of pathological bleeding and even death. In the case of such co-administration, INR and prothrombin time should be monitored.


Methotrexate.


Concomitant use of high doses of methotrexate (e.g., 300 mg) and PPIs has been reported to increase blood levels of methotrexate in some patients. Patients who use high doses of methotrexate, such as those with cancer or psoriasis, are advised to temporarily stop treatment with pantoprazole.


Other interactions.


Pantoprazole is largely metabolized in the liver through the cytochrome P450 enzyme system. the main metabolic pathway is demethylation by CYP2C19 and other metabolic pathways, including oxidation by the CYP3A4 enzyme. Studies with drugs that are also metabolized by these pathways, such as carbamazepine, diazepam, glibenclamide, nifedipine, and oral contraceptives containing levonorgestrel and Ethinyl Estradiol, have found no clinically significant interactions.


Interaction of pantoprazole with other drugs that are metabolized through the same enzyme system cannot be excluded.


The results of a number of studies on possible interactions indicate that pantoprazole does not affect the metabolism of active substances metabolized by CYP1A2 (for example, caffeine, theophylline), CYP2C9 (for example, Piroxicam, diclofenac, naproxen), CYP2D6 (for example, metoprolol), CYP2E1 (for example, ethanol), does not affect the P-glycoprotein, which provides digoxin absorption.


No interaction with concomitant antacids was detected.


Studies have been conducted on the interaction of pantoprazole with concomitantly prescribed certain antibiotics (clarithromycin, metronidazole, amoxicillin). No clinically significant interactions were found between these drugs.


Drugs that inhibit or induce CYP2C19.


CYP2C19 inhibitors, such as fluvoxamine, may increase the systemic effect of pantoprazole. Consideration should be given to reducing the dose of the drug for patients receiving long-term therapy with pantoprazole in high doses, and for patients with impaired liver function. Inducers of enzymes that affect CYP2C19 and CYP3A4, such as rifampicin and St. John's wort (Hypericum perforatum), can reduce plasma concentrations of PPIs that are metabolized through these enzyme systems.


Application features.


Impaired liver function. Patients with severe hepatic impairment should regularly monitor their liver enzyme levels, especially during long-term treatment. If the level of liver enzymes increases, treatment with the drug should be discontinued.


Combined use with NSAIDs.


The use of the drug Topraz, gastro-resistant tablets of 20 mg, for the Prevention of gastric and duodenal ulcers caused by taking NSAIDs for a long time should be limited to patients who are prone to frequent exacerbations of gastric and duodenal ulcers.


Risk assessment is based on individual risk factors, including age (> 65 years), a history of stomach or duodenal ulcers, and gastrointestinal bleeding.


Malignant neoplasms of the stomach. A symptomatic response to the use of pantoprazole may mask the symptoms of gastric malignancies and delay their diagnosis. If there are alarming symptoms (for example, in the case of significant weight loss, periodic vomiting, dysphagia, vomiting with blood, anemia, Melena), as well as if a stomach ulcer is suspected or present, the presence of a malignant process should be excluded.


If symptoms persist with adequate treatment, an additional examination is necessary.


HIV protease inhibitors. Concomitant use of pantoprazole with HIV protease inhibitors (such as atazanavir), whose absorption depends on intragastric ph, is not recommended due to a significant decrease in their bioavailability (see the section "interactions with other drugs and other types of interactions").


Absorption of vitamin B12. Pantoprazole may reduce the absorption of vitamin B12 (cyanocobalamin) due to the occurrence of hypo - and achlorhydria. This should be considered in the case of low body weight in patients or the presence of risk factors for reduced vitamin B12 uptake during long-term treatment, or the presence of appropriate clinical symptoms.


Long-term treatment. For long-term treatment, especially for more than one year, patients should be under regular medical supervision.


Gastrointestinal infections caused by bacteria. Treatment with the drug may slightly increase the risk of gastrointestinal infections caused by bacteria such as Salmonella and Campylobacter or Clostridium Difficile.


Hypomagnesemia. Cases of severe hypomagnesemia have been reported in patients treated with PPIs, such as pantoprazole, for at least 3 months, and in most cases for one year. The following serious clinical manifestations of hypomagnesemia may occur and initially develop unnoticed: fatigue, tetany, delirium, convulsions, dizziness, and ventricular arrhythmia. In the case of hypomagnesemia, in most cases, the condition of patients improved after replacement corrective therapy with magnesium preparations and discontinuation of PPIs.


Patients requiring long-term therapy, or patients taking PPIs concomitantly with digoxin or medications that may cause hypomagnesemia (such as diuretics), should have their magnesium levels determined before starting PPIs and periodically during treatment.


Bone fractures. Long-term treatment (more than one year) with high doses of PPIs may slightly increase the risk of hip, wrist, and spine fractures, mainly in the elderly or in the presence of other risk factors. Observational studies show that the use of PPIs can increase the overall risk of fractures by 10-40 %. Some of them may be caused by other risk factors. Patients at risk of developing osteoporosis should receive treatment in accordance with current clinical guidelines and consume sufficient amounts of vitamin D and calcium.


Subacute cutaneous lupus erythematosus. The use of PPIs is associated with very rare cases of subacute cutaneous lupus erythematosus. If a lesion occurs, especially in areas exposed to sunlight, and this is accompanied by arthralgia, the patient should immediately consult a doctor who will consider discontinuing the drug. The occurrence of subacute cutaneous lupus erythematosus in patients with previous PPI therapy may increase the risk of developing it with other PPI.


Influence on the results of laboratory tests.


Elevated levels of chromogranin a (CgA) may affect research results in the diagnosis of neuroendocrine tumors. To avoid such effects, treatment with the drug should be temporarily discontinued at least 5 days before the CGA level assessment (see the section "pharmacodynamics"). If CgA and gastrin levels do not return to normal after the initial measurement, repeated measurements should be performed 14 days after discontinuation of PPI treatment.


Excipients.


Tablets contain mannitol, which can have a mild laxative effect.


Use during pregnancy or lactation.


Pregnancy. Available data on the use of pantoprazole in pregnant women (approximately 300-1000 reports of pregnancy outcomes) indicate the absence of embryonic or FETO-neonatal toxicity of the drug. Reproductive toxicity has been observed in animal studies. As a precautionary measure, the use of the drug in pregnant women should be avoided.

Breast-feeding period. Animal studies have shown the excretion of pantoprazole in breast milk. There are insufficient data on the excretion of pantoprazole in human breast milk, but such excretion has been reported. The risk for newborns/infants cannot be excluded. The decision to stop breast-feeding or discontinue/abstain from treatment with the drug should be made taking into account the ratio of benefit from treatment to the mother/risk to the child.


Fertility. Pantoprazole did not affect fertility in animal studies.


Ability to influence the reaction rate when driving vehicles or other mechanisms.


Pantoprazole does not affect or has very little effect on the reaction rate when driving vehicles or other mechanisms. It is necessary to consider the possible development of adverse reactions, such as dizziness and visual disturbances. In such cases, you should not drive vehicles or work with other mechanisms.


Dosage and administration.


Topraz, gastro-resistant tablets, should be taken 1 hour before meals whole, not chewed or crushed, washed down with water.


Recommended dosage.


Adults and children over 12 years of age.


Symptomatic treatment of gastroesophageal reflux disease.


The recommended dose is 20 mg (1 tablet) of the drug Topraz per day. Usually, the symptoms of heartburn go away within 2-4 weeks. If this period is not enough, continue treatment for the next 4 weeks. After the symptoms disappear, the reappearance of symptoms can be controlled by applying 20 mg of the drug 1 time a day if necessary, taking 1 tablet when necessary. Switching to long-term therapy should be considered if satisfactory control of symptoms is not provided with therapy as needed.


Long-term treatment and Prevention of recurrent reflux esophagitis.


For long-term treatment, the maintenance dose is 20 mg (1 tablet) of the drug Topraz per day, with an exacerbation of the disease, it is possible to increase the dose to 40 mg per day. In this case, it is recommended to take Topraz 40 mg tablets. After the relapse is eliminated, the dose can be reduced again to 20 mg of the drug per day.


Adults.


Prevention of gastric and duodenal ulcers caused by non-selective nonsteroidal anti-inflammatory drugs (NSAIDs) in patients at risk who should take NSAIDs for a long time.


The recommended dose is 20 mg (1 tablet) of the drug Topraz per day.


Impaired liver function. Patients with severe hepatic impairment should not exceed the dose of 20 mg (1 tablet) per day.


Impaired renal function. Patients with impaired renal function do not need to adjust the dose.


Elderly patients do not need to adjust the dose.


Children. The drug is not recommended for use in children under 12 years of age, as data on the safety and efficacy of the drug for this age category are limited.


Overdose.


Symptoms of overdose are unknown.


Doses up to 240 mg administered intravenously for 2 minutes were well tolerated. Since pantoprazole binds extensively to proteins, it is not one of the drugs that can be easily eliminated by dialysis.


In case of overdose with the appearance of clinical signs of intoxication, symptomatic and supportive therapy is used. There are no recommendations for specific therapy.


Adverse reactions.


Adverse reactions can be expected in about 5% of patients. The most common adverse reactions were diarrhea and headache (occurring in about 1% of patients).


Undesirable effects are classified according to the frequency of occurrence into the following categories: very often (≥1/10), often (≥ 1/100 and          


For all adverse reactions reported during the post-marketing period, it is not possible to determine the frequency, so they are listed as "frequency unknown".


Within each frequency category, adverse reactions are listed in descending order of manifestations.


From the blood and lymphatic system.


Rare: agranulocytosis.


Very rare: leukopenia, thrombocytopenia, pancytopenia.


From the immune system.


Rare: hypersensitivity reactions (including anaphylactic reactions, anaphylactic shock).


From the side of metabolism and metabolism.


Rarely hyperlipidemia and increased lipid levels (triglycerides, cholestyrol), changes in body weight.


Unknown: hyponatremia, hypomagnesemia (see Section "application features"), hypocalcemia 1, hypokalemia. 


Mental disorders.


Infrequently: sleep disorders.


Rare: depression (including exacerbation).


Very rare: disorientation (including exacerbation).

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