Losec map pills film coated 20 mg N14
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Active ingredients
Omeprazole
Release form
Pills
Composition
1 tab. Omeprazole magnesium 20.6 mg, which corresponds to the content of omeprazole 20 mg Supplementary substances: microcrystalline cellulose - 220 mg, glyceryl monostearate (40-55) - 1.4 mg, hyprolosis - 4.8 mg, hypromellose - 15 mg, magnesium stearate - 0.7 mg, copolymer methacrylic and ethacrylic acids - 27 mg, paraffin - 0.2 mg, macrogol - 2.5 mg, polysorbate 80 - 0.1 mg, crospovidone - 4.6 mg, sodium fumarate - 0.5 mg, sucrose spherical granules - 22 mg, talc - 8.3 mg, titanium dioxide ( E171) - 2.2 mg, triethyl citrate - 8.2 mg, iron dye red oxide (E172) - 0.03 mg.
Pharmacological effect
The mechanism of action of omeprazole is a weak base. Concentrates in the acidic environment of the secretory tubules of the parietal cells of the gastric mucosa, is activated and inhibits the proton pump - the enzyme H +, K + -ATPase. The effect of omeprazole on the last stage of the formation of hydrochloric acid in the stomach is dose-dependent and provides highly effective inhibition of basal and stimulated secretion of hydrochloric acid, regardless of the stimulating factor. The effect on the secretion of gastric juices of MAPS with daily oral administration provides rapid and effective inhibition of day and night secretion of hydrochloric acid. The maximum effect is achieved within 4 days of treatment. In patients with duodenal ulcer Losec Mups 20 mg causes a steady decrease in 24-hour gastric acidity of at least 80%. When this is achieved, the average maximum concentration of hydrochloric acid is reduced by 70% within 24 hours after stimulation with pentagastrin. In patients with duodenal ulcer Losec Mups 20 mg, with daily oral administration, maintains the pH value in the intragastric medium at a pH of> 3 on average for 17 hours per day. Inhibition of the secretion of hydrochloric acid depends on the area under the concentration-time curve (AUC) of omeprazole, and not on the plasma concentration of the drug at a given time. Effect on Helicobacter pyloriOmep azole has a bactericidal effect on Helicobacter pylori in vitro. Eradication of Helicobacter pylori when using omeprazole together with antibacterial agents is accompanied by rapid elimination of symptoms, a high degree of healing of defects of the mucous membrane of the gastrointestinal tract, and long-term remission of peptic ulcer, which reduces the likelihood of bleeding as well as constant maintenance therapy. Other effectsassociated with the inhibition of the secretion of hydrochloric acid in patients taking drugs that lower the secretion of the gastric glands for a long period of time, more often marked the formation of glandular cysts in the stomach; benign cysts and pass independently on the background of continued therapy. These phenomena are due to physiological changes as a result of inhibition of the secretion of hydrochloric acid. Reducing the secretion of hydrochloric acid in the stomach under the action of proton pump inhibitors or other drugs that reduce the acidity of the stomach increases the growth of the normal intestinal microflora, which in turn can lead to a slight increase in the risk of developing intestinal infections caused by bacteria of the genus Salmonella spp. and Campylobacter spp., and in hospitalized patients, probably also the bacterium Clostridium difficile. During treatment with drugs that lower the secretion of the gastric glands, the concentration of gastrin in the serum is elevated. Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (CgA) increases. Increasing the CgA concentration may influence the results of examinations for the detection of neuroendocrine tumors. To prevent this effect, treatment with proton pump inhibitors should be suspended 5-14 days prior to the study of CgA concentration. If during this time the CgA concentration did not return to normal, the study should be repeated. Children and adult patients who took omeprazole for a long time showed an increase in the number of enterochromaffin-like cells, probably due to an increase in serum gastrin concentration. This phenomenon has no clinical significance.
Pharmacokinetics
Distribution Omeprazole is absorbed in the small intestine, usually within 3-6 hours. Bioavailability after oral administration is approximately 60%. Food intake does not affect the bioavailability of omeprazole. The indicator of the connectivity of omeprazole with plasma proteins is about 95%, the volume of distribution is 0.3 l / kg. Metabolism Omeprazole is completely metabolized in the liver. The main enzymes involved in the metabolic process are CYP2C19 and CYP3A4. The resulting metabolites - sulfone, sulfide and hydroxy-omeprazole do not have a significant effect on the secretion of hydrochloric acid. The total plasma clearance is 0.3-0.6 l / min.The bioavailability of omeprazole increases by approximately 50% when taken again as compared to taking a single dose. Excretion of T1 / 2 is about 40 minutes (30-90 minutes). About 80% is excreted in the form of metabolites by the kidneys, and the rest - by the intestine.
Indications
Losec Mups is intended for the treatment of the following diseases: - duodenal ulcer; - gastric ulcer; - NSAID associated ulcers and erosions of the stomach and duodenum; - ester of Helicobacter pylorrhea in peptic ulcer; associated with increased acidity; - Zollinger-Ellison syndrome.
Contraindications
- known hypersensitivity to omeprazole, substituted benzimidazoles or other ingredients that make up the drug. With caution If you have symptoms such as significant spontaneous weight loss, frequent vomiting, dysphagia, blood vomiting or melena, as well as stomach ulcers (or suspected stomach ulcer) should exclude the presence of a malignant neoplasm, because treatment can lead to masking of the symptoms and, thus, delay the diagnosis.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
Studies have shown no side effect of omeprazole on the health of pregnant women, on the fetus or on the newborn. Losec Mups can be used during pregnancy. Omeprazole penetrates into breast milk, however, when used in therapeutic doses of exposure to the child is unlikely.
Dosage and administration
Inside Tablets Losec Mups is recommended to take in the morning, the tablet should be swallowed whole with a liquid. Tablets can not be chewed or crushed. Tablets can be dissolved in water or slightly acidified liquid, for example, in fruit juice. The resulting solution should be used within 30 minutes.To be sure of taking the full dose, pour half the liquid back into the glass, shake it up and drink. Duodenal ulcer Patients with an active duodenal ulcer are advised to take Losec MAPS 20 mg 1 time per day. The drug provides rapid elimination of symptoms. In most patients, ulcer healing occurs within 2 weeks. In cases where complete healing of the ulcer does not occur within 2 weeks, healing is achieved with the subsequent 2-week intake of the drug Losec Mups.Patients with a duodenal ulcer, little susceptible to treatment, are usually prescribed Losec Mups 40 mg 1 time day; ulcer healing usually occurs within 4 weeks. To prevent relapse, Losec MAPS 10 mg is recommended 1 time per day for patients with a duodenal ulcer. If necessary, the dose can be increased to 20-40 mg 1 time per day. Gastric ulcer. Recommended dose - Losec Mups 20 mg 1 time per day. The drug provides rapid elimination of symptoms. In most patients, the cure occurs within 4 weeks. In those cases, when after the first course of taking the drug, complete healing does not occur, a repeated 4-week course of treatment is usually prescribed, during which healing is achieved. Patients with a gastric ulcer who are not very susceptible to treatment are usually prescribed Losec MAPS 40 mg 1 time per day. ; healing is usually achieved within 8 weeks. To prevent recurrence, Losec MAPS 20 mg is recommended 1 time per day in patients with a stomach ulcer. If necessary, the dose can be increased up to 40 mg 1 time per day. NSAIDs associated ulcers and erosions of the stomach and duodenum 1 time per day. The drug provides rapid elimination of symptoms, in most patients, the cure occurs within 4 weeks. In those patients who did not cure during the initial therapy period, healing is usually achieved with repeated 4-week intake of the drug. The dose of Losec Mups is recommended for the prevention of ulcers and erosions of the stomach and duodenal ulcers and dyspepsia symptoms associated with the intake of NSAIDs - 20 mg 1 time per day. Helicobacter pylori eradication regimes for peptic ulcer. Three-component treatment regimen: Losec Mups 20 mg, amoxicillin 1 g and clarithromycin 500 mg.All drugs are taken 2 times a day for one week or Losec Mups 20 mg, metronidazole 400 mg (or tinidazole 500 mg) and clarithromycin 250 mg. All drugs are taken 2 times a day for one week or Losec Mups 40 mg 1 time per day, as well as amoxicillin 500 mg and metronidazole 400 mg 3 times a day for one week. Two-part treatment regimen: Losec Mups 40-80 mg daily and amoxicillin 1.5 g daily (the dose should be divided into parts) for two weeks. During clinical trials, amoxicillin was used in a daily dose of 1.5-3 g, Losec Mups 40 mg 1 time per day and Clarithromycin 500 mg 3 times a day for two weeks. To ensure complete healing, further treatment is carried out in accordance with the recommendations in the sections of the Ulcer. duodenal ulcer and gastric ulcer. In cases where after undergoing a course of treatment a test for Helicobacter pylori remains positive, the treatment can be repeated. Reflux esophagitis The recommended dose is one tablet of Losec Mups 20 mg 1 time per day. The drug provides rapid elimination of symptoms. In most patients, the cure occurs within 4 weeks. In those cases when after the first course of taking the drug a complete cure does not occur, a repeated 4-week course of treatment is usually prescribed, during which the cure is achieved. Losec Mups 40 mg is recommended 1 day per day for patients with severe reflux of the esophagitis; Cure usually occurs within 8 weeks. Patients with reflux esophagitis in remission are prescribed Losec MAPS 10 mg 1 time per day as long-term courses of maintenance therapy. If necessary, the dose can be increased to 20-40 mg. Symptomatic gastroesophageal reflux disease. The recommended dose is Losec Mups 20 mg 1 time per day. The drug provides rapid elimination of symptoms. The therapeutic effect can be achieved with a daily dose of 10 mg, therefore, individual selection of the dose is not excluded. If after 4 weeks of treatment (Losek MAPS 20 mg 1 time per day) the symptoms do not disappear, additional examination of the patient is recommended. Dispepsia associated with hyperacidity In order to relieve pain and / or eliminate discomfort in the epigastric region, with heartburn or without heartburn, Losek is prescribed MAPS 20 mg 1 time per day. The therapeutic effect can be achieved with a dose of 10 mg 1 time per day, so treatment can begin with this dose.If after 4 weeks of treatment (Losek MAPS 20 mg 1 time per day) the symptoms do not disappear, additional examination of the patient is recommended. Zollinger-Ellison syndrome For patients with Zollinger-Ellison syndrome, the drug is prescribed in an individual dosage. Treatment continues on clinical indications as long as necessary. The recommended starting dose is Losec MAPS 60 mg daily. In all patients with a severe form of the disease, as well as in cases when other therapeutic methods did not lead to the desired result, the use of the drug was effective in more than 90% of patients when taking 20-120 mg of Losec Mups daily. In cases where the daily dose of the drug exceeds 80 mg, the dose should be divided into two parts and taken 2 times a day. Impaired renal function For patients with impaired renal function, dose adjustment is not required. Impaired liver function In patients with impaired liver function, bioavailability and half-life in plasma omeprazole increase. In this regard, a dose of 10-20 mg per day is sufficient. Elderly patients For elderly patients, dose adjustment is not required. Children Use experience in children is limited.
Side effects
Below are the side effects that do not depend on the dosing regimen of omeprazole, which were noted during clinical studies, as well as during post-marketing use. Often (> 1/100, <1/10) Headache, abdominal pain, diarrhea, flatulence, nausea / vomiting, constipationFrequently (> 1/1000, <1/100) Dermatitis, pruritus, rash, urticaria, drowsiness, insomnia, dizziness, paresthesias, malaise, increased activity of liver enzymesRedko (> 1/10000, <1/1000) Hypersensitivity reactions (eg fever, angioedema, anaphylactic reaction / anaph ilaktichesky shock), bronchospasm, hepatitis (with jaundice or without), liver insufficiency, encephalopathy in patients with liver disease, arthralgia, myalgia, muscle weakness, leukopenia, thrombocytopenia, agranulocytosis, pancytopenia, depression, hyponatremia, agitation, aggression, confusion, hallucinations , taste disturbance, blurred vision, dry mouth, stomatitis, gastrointestinal candidiasis, alopecia, photosensitization, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis,interstitial nephritis, gynecomastia, sweating, peripheral edema, microscopic colitis. Very rare (<1/10000) time; benign cysts and pass independently on the background of continued therapy.
Overdose
Single oral doses of the drug Losec MAPS up to 400 mg did not cause any severe symptoms. When taken by adults, 560 mg of omeprazole showed moderate intoxication. With increasing doses, the rate of drug elimination did not change (first order kinetics), specific treatment was not required. Symptoms: dizziness, confusion, apathy, headache, vascular dilatation, tachycardia, nausea, vomiting, flatulence, diarrhea. Treatment: symptomatic treatment if necessary, gastric lavage, the appointment of activated carbon.
Interaction with other drugs
The effect of omeprazole on the pharmacokinetics of other drugs Reducing the secretion of hydrochloric acid in the stomach during treatment with omeprazole and other proton pump inhibitors may reduce or increase the absorption of other drugs, the absorption of which depends on the acidity of the environment. Like other drugs that reduce the acidity of gastric juice, treatment with omeprazole may result to a decrease in the absorption of ketoconazole, itraconazole and erlotinib, as well as an increase in the absorption of drugs such as digoxin. The joint omeprazole at a dose of 20 mg once a day and digoxin increases the bioavailability of digoxin by 10% (digoxin bioavailability increased by up to 30% in 20% of patients). It was shown that omeprazole interacts with some antiretroviral drugs. The mechanisms and clinical significance of these interactions not always known. Increasing the pH value during omeprazole therapy may affect the absorption of antiretroviral drugs. Interaction at the level of an isoenzyme CYP2C19 is also possible. With the joint use of omeprazole and some antiretroviral drugs, such as atazanavir and nelfinavir, a decrease in their concentration in serum is observed during therapy with omeprazole.In this regard, the combined use of omeprazole with antiretroviral drugs such as atazanavir and nelfinavir is not recommended. With simultaneous use of omeprazole and saquinavir, an increase in the concentration of saquinavir in serum was observed, when used with some other antiretroviral drugs, their concentration did not change. the main isoenzyme involved in its metabolism. Combined use of omeprazole with other drugs that are involved in the metabolism of CYP2C19 isoenzyme, such as diazepam, warfarin (R-warfarin) or other vitamin K antagonists, phenytoin and Cilostazol, can slow down the metabolism of these drugs. It is recommended that patients taking phenytoin and omeprazole be monitored, and phenytoin dose reduction may be necessary. However, concomitant treatment with omeprazole at a daily dose of 20 mg does not affect the concentration of phenytoin in the blood plasma of patients who take the drug for a long time. When omeprazole is used by patients receiving warfarin or other vitamin K antagonists, monitoring of the international normalized ratio is necessary; in some cases, a reduction in the dose of warfarin or another vitamin K antagonist may be necessary. At the same time, concomitant treatment with omeprazole at a daily dose of 20 mg does not change the coagulation time in patients who take warfarin for a long time. The use of omeprazole at a dose of 40 mg once a day resulted in to an increase in Cmax and AUC of Cilostazol by 18% and 26%, respectively; for one of the active metabolites of Cilostazol, the increase was 29% and 69%, respectively. According to the research results, pharmacokinetic / pharmacodynamic interaction between clopidogrel (loading dose 300 mg and maintenance dose 75 mg / day) and omeprazole (80 mg / day inside) is observed, which leads to a decrease in the active metabolite of clopidogrel, by an average of 46% and reduce the maximum inhibition of ADP-induced platelet aggregation, on average, by 16%. The clinical significance of this interaction is not clear. Increased risk of cardiovascular complications with the combined use of clopidogrel and proton pump inhibitors, including omeprazole,It was not shown in a prospective randomized, incomplete study involving more than 3,760 patients receiving placebo or omeprazole at a dose of 20 mg / day concurrently with clopidogrel and acetylsalicylic acid (ASA) therapy, and was not confirmed by an additional non-randomized analysis of the clinical outcomes of large-scale randomized cancer surveys. . The results of a number of observational studies are controversial and do not give a definite answer about the presence or absence of an increased risk of tro cardiovascular complications associated with the combined use of clopidogrel and proton pump inhibitors. When clopidogrel was used in conjunction with a fixed combination of 20 mg of esomeprazole and 81 mg of ASK, the exposure to clopidogrel kaktivnom metabolite decreased by almost 40% compared to clopidogrel monotherapy with the maximum heart rate. induced platelet aggregation were the same, which is probably due to simultaneous administration of ASA at a low dose. Omeprazole does not affect the metabolism of drugs CYP3A4 isoenzyme metabolized, such as cyclosporine, lidocaine, quinidine, estradiol, erythromycin, and budesonide. Omeprazole has not been interacted with the following drugs: caffeine, theophylline, S-warfarin, piroxicam, diclofenac, naproxen, metoprol, Icropol, Metoprol, Icopol, Icoprale, S-warfarin, Piroxicam, Diclofenac, Naproxol, Metoprol, and Icopol, can be used as the drug. simultaneous use of omeprazole and tacrolimus, an increase in serum tacrolimus concentration was noted. In some patients, an increase in the concentration of methotrexate was noted against the background of joint use with proton pump inhibitors. When prescribing high doses of methotrexate, the possibility of temporary discontinuation of omeprazole should be considered. Effect of drugs on the pharmacokinetics of omeprazole The isoenzymes СYP2C19 and СYP3 А4 are involved in the metabolism of omeprazole. The combined use of omeprazole and CYP2C19 and CYP3A4 isoenzyme inhibitors, such as clarithromycin and voriconazole, can lead to an increase in plasma plasma concentration of omeprazole by slowing down the metabolism of omeprazole. The combined use of voriconazole and omeprazole leads to a more than twofold increase in the AUC of omeprazole.Due to the good tolerability of high doses of omeprazole, short-term joint use of these drugs does not require correction of the dose of omeprazole. blood plasma by accelerating the metabolism of omeprazole.
special instructions
If there are any alarming symptoms (for example, such as significant spontaneous weight loss, recurrent vomiting, dysphagia, vomiting with blood or melena), as well as in the presence of a stomach ulcer (or if a stomach ulcer is suspected), the presence of a malignant neoplasm should be excluded, since drug treatment Losec Mups can lead to a smoothing of symptoms and delay the diagnosis. It is not recommended to use omeprazole together with drugs such as atazanavir and nelfinavir. pharmacokinetic / pharmacodynamic interaction between clopidogrel (loading dose 300 mg and maintenance dose 75 mg / day) and omeprazole (80 mg / day inside), which leads to a decrease in the active metabolite of clopidogrel by an average of 46% and a decrease in the maximum inhibition of ADP induced platelet aggregation by an average of 16%. Therefore, the simultaneous use of omeprazole and clopidogrel should be avoided. Separate observational studies indicate that proton pump inhibitor therapy may slightly increase the risk of osteoporosis-related fractures, but in other similar studies there is no increase in risk. In randomized, double-blind, controlled clinical trials of omeprazole and esomeprazole, including two open-label studies with a therapy duration of more than 12 years, did not confirm the association of fractures against theoproposis with proton pump inhibitors. Although the cause-and-effect relationship of omeprazole / esomeprazole with fractures against osteoporosis has not been established, patients at risk of developing osteoporosis or fractures against its background should be under appropriate clinical observation. Effect on ability to drive a car or other mechanisms There are no data on the effect of the drug Losec Mups on the ability to drive a car or other mechanisms.However, due to the fact that during therapy dizziness, blurred vision and drowsiness may occur, care should be taken when driving vehicles or other mechanisms.