1 tablet contains pantoprazole sodium sesquihydrate equivalent to pantoprazole 20mg
other ingredients:sodium carbonate anhydrous, beckons (E 421), crospovidone, hydroxypropyl cellulose, calcium stearate, Eudragit L30D55, triethylcitrate, sodium lauryl sulfate, titanium dioxide (E 171), iron oxide yellow (E172), talc, Opadry white 03F58750 *.
* Opadry 03F58750 white: hypromellose, titanium dioxide (E 171), polyethylene glycol, talc.The
Tablet coated liner.
basic physico-chemical properties:oval biconvex tablets coated in yellow.The
preparations for the treatment of acid-dependent diseases. Proton pump inhibitor.
code ATX a02b C02.The
Mechanism of action.
the Pantoprazole is a substituted benzimidazole which inhibits the secretion of hydrochloric acid in the stomach by specific blockade of the proton pumps of parietal cells. Pantoprazole is transformed into an active form in an acidic environment in parietal cells, where it inhibits the enzyme H+-K+-Atphase, that is, it blocks the final stage of hydrochloric acid production in the stomach. The inhibition is dose-dependent and inhibits 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 (IPP) and inhibitors H2receptors, reduces acidity in the stomach and thus increases gastrin secretion in proportion to the decrease in acidity. Increasing gastrin secretion is reversible. Since pantoprazole binds to the enzyme distal relative to the cell receptor, it can inhibit hydrochloric acid secretion independently of stimulation by other substances (acetylcholine, histamine, gastrin). The effect of oral and intravenous use is the same.
the use of pantoprazole increased fasting gastrin. In short - term use, the level of gastrin in most cases does not exceed the upper limit of the norm. With long - term treatment of gastrin levels in most cases grow twice. Excessive increase, however, occurs only in rare cases. As a result, sometimes with prolonged treatment, there is a weak or moderate increase in specific endocrine (ECL) cells in the stomach (like adenomatoid hyperplasia). However, to date, there is no data on the creation of human cells-predecessors of neuroendocrine tumors (atypical hyperplasia) or neuroendocrine tumors of the stomach. Taking into account the published data, it is impossible to completely exclude the effect of long-term (more than one year) treatment with pantoprazole on the endocrine parameters of the thyroid gland.
the Pantoprazole is rapidly absorbed and maximum concentration in plasma achieved after a single oral dose of 20 mg. In an average 2-2. 5 hours after intake maximum concentration in the serum at a level of about 1-1,5 µg/ml concentration remains constant after repeated administration. Pharmacokinetic properties do not change after a single or repeated administration. In the dose range from 10 to 80 mg pharmacokinetics pantoprazole in plasma remains linear as oral administration and intravenous. It was found that the bioavailability of tablets is about 77%. Simultaneous eating does not affect AUC (the area under the plasma concentration - time curve) or the maximum serum concentration, and therefore bioavailability. Simultaneous food intake increases only the variance of the latent period.
Binding of pantoprazole to plasma proteins is about 98%. The volume of distribution is about 0,15 l/kg.
Metabolism.the Substance is metabolized almost exclusively in the liver. The main metabolic pathway is demethylation by CYP2C19 followed by sulfur conjugation; in other metabolic pathways, oxidation by CYP3A4 belongs.
Output.the Ultimate half-life is about 1:00, and clearance - 0,1 l/h/kg. there have Been several instances of delay of the output. Due to specific binding of pantoprazole with proton pump of parietal cells, the half-life period does not correspond to much longer duration of action (inhibition of acid secretion).
the Main part of metabolites of pantoprazole is excreted in urine (about 80%), the rest is excreted in feces. The main metabolite in serum and urine desmethyldonepezil conjugated with sulfate. The half-life of the primary metabolite (about 1.5 hours) slightly exceeds the half-life of pantoprazole.
Special patient groups.
Slow metabolizers.in about 3% of Europeans there is a need for a functionally active enzyme CYP2C19; they are called slow metabolizers. In the organisms of such persons metabolism pantoprazole, probably mainly catalyzed by the enzyme CYP3A4. After taking one dose of 40 mg pantoprazole average area, limited pharmacokinetic curve "concentration in plasma-time", was about 6 times higher in slow metabolizers than in persons with functionally active enzyme CYP2C19 (fast metabolizers). The maximum concentration in plasma increased by about 60%. These results do not affect the dosage of pantoprazole.
impairment of renal function.recommendations for dose reduction in the appointment of pantoprazole patients with impaired renal function (including patients on dialysis) no. Like healthy people, they have a short half-life of pantoprazole. Only very small amounts of pantoprazole are dialyzed. Despite the fact that the main metabolite moderately long half-life (2-3 hours), the conclusion is still fast, so the cumulation does not occur.
liver dysfunction. Although patients with liver cirrhosis (classes A and B on a scale child-Pugh) the half-life increases up to 3-6 hours, and AUC is increased 3 to 5 times the maximum serum concentration increases only slightly - by 1.5 times compared to healthy volunteers.
elderly Patients.a Slight increase in AUC and Cmaxin elderly patients compared to younger patients is not clinically significant.
After a single oral dose of 20 or 40 mg of oral pantoprazole AUC and Cmaxranging in age from 5 to 16 years were in the range of those in adults.
Adults and children over 12 years of age.
Symptomatic treatment of gastroesophageal reflux disease.
Long-term treatment and prevention of relapse reflux esophagitis.
Prevention of formation of gastric ulcer and duodenal ulcer caused by taking non-selective non-steroidal anti-inflammatory drugs (NSAIDs) in patients at risk, should use NSAIDs for a long time.
hypersensitivity to the active substance, benzimidazole derivatives or any component of the drug.The
the effect of pantoprazole on the absorption of other drugs. 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).
drugs against HIV (atazanavir). The joint use of IPP with atazanavir and other HIV drugs, the adsorption of which depends on pH, can lead to a significant reduction in the bioavailability of the latter and affect their effectiveness. Therefore, the combined use of PPIS with atazanavir is not recommended.
Indirect anticoagulants (warfarin and phenprocoumon).Although there is no sufficient data about interaction with concomitant administration of pantoprazole with phenprocoumon and warfarin, patients who use anticoagulants, it is recommended to monitor PV/PIM (international normalizing an index) after the commencement, termination or during irregular intake of pantoprazole.
Methotrexate.concomitant use of high doses of methotrexate (e.g. 300 mg) and proton pump inhibitors has been Reported to increase blood methotrexate levels in some patients. Patients taking high doses of methotrexate, such as cancer patients or psoriasis, are recommended to temporarily discontinue treatment with pantoprazole.
other interactions.Pantoprazole is highly metabolized in the liver through the cytochrome P450 enzyme system. The main pathway is demethylation via 2C19 and other metabolic pathways, including oxidation by the enzyme СУРЗА4. No data on clinically significant interactions between pantoprazole and the drugs that also are metabolized via these pathways (carbamazepine, diazepam, glibenclamide, nifedipine, phenprocoumon, oral contraceptives containing levonorgestrel and ethinyl estradiol). It is known that pantoprazole does not affect the metabolism of active substances metabolised via CYP1A2 (such as caffeine, theophylline), CYP2C9 (e.g., piroxicam, diclofenac, naproxen), CYP2D6 (such as metoprolol), СУР2Е1 (such as ethanol). Also, the pantoprazole does not affect p-glycoprotein, which ensures the absorption of digoxin.
there was No interaction with simultaneously appointed by the antacids.
there is no evidence of clinically significant interactions between pantoprazole and simultaneously prescribed certain antibiotics (clarithromycin, metronidazole, amoxicillin).
liver dysfunction. Patients with severe liver dysfunction should regularly monitor the level of liver enzymes. In case of increasing the level of liver enzymes, treatment should be stopped.
Combination therapy.in combination therapy, follow the instructions for the use of appropriate medicines.
the combined use with NSAIDs.
Long-term use of the drug Zolopanttablets 20 mg for the prevention of gastric ulcers and duodenal ulcers caused by NSAIDs should be restricted in patients prone to frequent exacerbations of ulcers of the stomach and duodenum.
Assessment of risk level takes into account individual risk factors, including age (> 65 years), history of development of gastric ulcer or duodenal ulcer and gastrointestinal bleeding.
anxiety symptoms available.in the presence of anxiety symptoms (for example, in the case of significant weight loss, periodic vomiting, dysphagia, vomiting with blood, anemia, melena), as well as in the case of suspected gastric ulcer or gastric ulcer, it is necessary to exclude malignancy, since the treatment of pantoprazole can mask the symptoms of malignant ulcers and delay diagnosis. If symptoms persist further adequate treatment, it is necessary to continue the study.
Joint application with atazanavir. Proton pump inhibitors are not recommended for use in conjunction with atazanavir (see section "Interaction with other drugs and other types of interactions"). If the combination of Zolopentwith atazanavir is necessary, careful clinical monitoring (e.g. viral load measurement) should be carried out in combination with an increase in the dose of atazanavir to 400 mg with 100 mg of ritonavir. The dose of pantoprazole is 20 mg per day should not be exceeded.
absorption of vitamin B12. In patients with hypersecretory pathological conditions in need of long - term treatment, pantoprazole, like all drugs that block the production of hydrochloric acid, can reduce the absorption of vitamin b12(cyanocobalamin) in connection with the emergence of Hypo-and ahlorgidrii. This should be taken into account in patients with reduced body weight or risk factors for vitamin b uptake in12in long-term treatment, or the presence of appropriate clinical symptoms.
Long-term treatment.after a long period of treatment, especially for more than a year, patients should be under constant medical supervision.
infections of the gastrointestinal tract caused by bacteria.Pantoprazole, like other proton pump inhibitors, can increase the number of bacteria that are usually present in the upper gastrointestinal tract. Treatment with the drug may slightly increase the risk of gastrointestinal infections caused by bacteria such asSalmonellaandCampylobacterorC. Difficult.
Hypomagnesemia.there have been cases of severe hypomagnesemia in patients treated with PPIS like pantoprazole for at least three months, and in most cases during the year. May arise and to quietly develop the next major clinical manifestations of hypomagnesaemia include 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 and discontinuation of IPP.
patients in need of long-term therapy, or patients who take STIs in combination with digoxin or drugs that may cause hypomagnesemia (e.g. diuretics), need to determine the level of magnesium before starting treatment of STIs and periodically during treatment.
fractures of bones.Long-term treatment (more than 1 year) with high doses of proton pump inhibitors may slightly increase the risk of fracture of hip, wrist and spine, especially in the elderly or in the presence of other risk factors. It is known that the use of proton pump inhibitors can increase the overall risk of fractures by 10-40%. Patients at risk of osteoporosis should receive treatment in accordance with the current clinical guidelines and consume sufficient vitamin d and calcium.
use during pregnancy or lactation.
Pregnancy.experience with the use of pantoprazole in pregnant women is limited. There is evidence about the presence of pantoprazole embryotoxicity. The potential risk to humans is unknown. The drug should not be used during pregnancy, except in cases of emergency.
breastfeeding.Pantoprazole is excreted in human breast milk. The decision to stop breastfeeding or discontinue/abstain from treatment Zolopantmust take into account the benefit of breast feeding for the child and benefits Zolopantfor women.
Ability to influence the reaction rate when driving motor transport or operating other mechanisms.
it is Necessary to take into account the possible development of adverse reactions such as dizziness and blurred vision. In such cases, you should not drive vehicles or work with other mechanisms.
Zolopant20 mg should be taken 1:00 to food whole without chewing but not grind with water.
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 Zolopantper day. Usually, the symptoms of heartburn occur within 2-4 weeks. If this period is not enough, the treatment continues for the next 4 weeks. After the symptoms disappear, its recurrence can be controlled using 20 mg, depending on the need.
Long-term treatment and prevention of relapse reflux esophagitis.
for long-term treatment, the maintenance dose is 20 mg (1 tablet) of the drug Zolopentper day, with an exacerbation of the disease, the dose may increase to 40 mg per day. In this case, we recommend taking the tablets Zolopant40 mg. After elimination of the relapse the dose can be reduced again to 20 mg per day.
Prevention of gastric ulcers and duodenal ulcers caused by taking non-selective non-steroidal anti-inflammatory drugs (NSAIDs) in patients at risk need to take NSAIDs for a long time.
the recommended dose is 20 mg (1 tablet) of the drug Zolopantper day.
patients with impaired liver function. Patients with severely impaired liver function should not exceed a dose of 20 mg (1 tablet) per day.
Patients with impaired renal function.patients with impaired renal function do not require dose adjustment.
elderly Patientsdose adjustment is not required.
Children.the Drug is not recommended for children under 12 years of age as the safety and efficacy data for this age group are limited.
the Symptoms of an overdose are unknown.
Doses up to 240 mg when administered intravenously within 2 minutes was well tolerated. Pantoprazole is extensively bound to proteins, not completely excreted by dialysis.
in case of overdose with clinical signs of intoxication, symptomatic and supportive therapy is used. There are no recommendations for specific therapy.
from blood and lymphatic system: agranulocytosis, leukopenia, thrombocytopenia, pancytopenia.
from the immune system: hypersensitivity reactions (including anaphylactic reactions, anaphylactic shock).
Metabolism and metabolic disorders: hyperlipidemia and increased lipid levels (triglycerides, cholesterol), changes in body weight, hyponatremia, hypomagnesemia.
on the part of the psyche: sleep disorders, depression (including exacerbations), disorientation (including exacerbations), hallucinations, confusion (especially in patients with a predisposition to these disorders, as well as exacerbation of these symptoms if they exist).
nervous system:headache, dizziness, taste disorders, paresthesia.
on the part of organs of sight: blurred vision/blurred vision.
from the digestive tract: diarrhea, nausea, vomiting, bloating, constipation, dry mouth, abdominal pain and discomfort.
from the digestive system: increased levels of liver enzymes (transaminase, g-GT), increased levels of bilirubin, hepatocyte lesions, jaundice, hepatocellular insufficiency.
skin and subcutaneous tissue:skin rash, exanthema, itching, urticaria, angioedema, Stevens-Johnson syndrome, Lyell syndrome, multiform erythema, photosensitization.
on the part of the musculoskeletal system and connective tissue: hip fracture, wrist or spine arthralgia, myalgia, muscle spasm.
on the part of the kidneys and urinary system: interstitial nephritis (with the possible development of renal failure).
side reproductive system and mammary glands: gynecomastia.
Common disorders: asthenia, fatigue, malaise, fever, peripheral edema.The
Store in its original packaging at a temperature not exceeding 25 ° C.
keep out of reach of children.The
For 14 tablets in a blister. 1 blister in a cardboard box.The
According to the recipe.The
LLC "Kusum Pharm".
Ukraine, 40020, M. Sumi, 54, Skryabina str.
Zolopent tablets 20 mg No. 14 – a pharmaceutical agent for the treatment of peptic ulcer, which acts as an active proton pump inhibitor. The therapeutic effect is achieved with the first dose. The active ingredient is pantoprazole. Component blocks the final phase of secretion of hydrochloric acid exhibits antibacterial, anti-Helicobacter effect. The exposure duration is 24 hours. Shown for use with:
After the initial oral use is quickly absorbed. The total bioavailability is 77%.
the Optimal rate depends on the type and severity of the disease, the presence of comorbidities and is determined by a specialist after a preliminary examination of the gastrointestinal tract. The recommended dose for adults is a tablet (20 mg) once a day. In some situations, the norm can be increased to 40 milligrams. The drug is contraindicated in pregnancy, hepatitis, cirrhosis, liver failure, hypersensitivity to certain components. It is not recommended to take the medicine simultaneously with atazanavir, ketoconazole, enzymes.