Losek MAPS of 20 mg

General characteristics. Structure:

Each tablet contains:
tablets of 20 mg:
Active agent: омепразол magnesium of 20,6 mg (equivalent 20 mg of an omeprazol).
Excipients: cellulose of microcrystallic 220,0 mg, glyceryl mg monostearate (40-55) 1,4, a hypro rod of 4,8 mg, a gipromelloz of 15,0 mg, magnesium stearate of 0,7 mg, methacrylic and etakrilovy acids copolymer of 27,0 mg, paraffin of 0,2 mg, a macrogoal of 2,5 mg, mg polysorbate (80) 0,1, кросповидон 4,6 mg, sodium of the stearylfumarating 0,5 mg, sucrose spherical granules of 22,0 mg, talc of 8,3 mg, titanium dioxide (E171) of 2,2 mg, triethyl citrate of 8,2 mg, dye ferrous oxide red (E172) of 0,3 mg.
DESCRIPTION
tablets of 10 mg: an oblong biconvex tablet of light pink color, film coated, with I0 mG engraving on one party and a badge -
on other party.
tablets of 20 mg: an oblong biconvex tablet of pink color, film coated, with an engraving of 20 mG on one party and a badge -
on other party.

Pharmacological properties:

Pharmacodynamics. Action mechanism
Omeprazol is the weak basis. Concentrates in acid medium of secretory tubules of covering cells of a mucous membrane of a stomach, it is activated and inhibits the proton pump – H+, K enzyme +-Atfazu. Influence of an omeprazol on the last stage of process of formation of hydrochloric acid in a stomach is dozozavisimy and provides highly effective inhibition of basal and stimulated secretion of hydrochloric acid irrespective of the stimulating factor.
Influence on secretion of a gastric juice of Losek® МАПС® at daily oral administration provides bystry and effective inhibition of day and night secretion of hydrochloric acid. The maximum effect is reached within 4 days of treatment. With an ulcer of a duodenum of Losek® of МАПС® 20 mg causes steady decrease in 24-hour gastric acidity in patients not less than for 80%. At the same time decrease in average maximum concentration of hydrochloric acid after stimulation by Pentagastrinum for 70% within 24 hours is reached. At patients with an ulcer of a duodenum of Losek® of МАПС® 20 mg at daily oral administration maintains in the intragastric environment value of acidity at the level of pH3 on average within 17 hours a day. The inhibition of secretion of hydrochloric acid depends on the area under a curve concentration - time (AUC) of an omeprazol, but not on concentration of drug in plasma of time at present.
Action on Helicobacter pylori
Omeprazol has bactericidal effect on Helicobacter pylori in vitro. Eradikation Helicobacter pylori at use of an omeprazol together with antibacterial agents is followed by bystry elimination of symptoms, high extent of healing of defects of a mucous membrane of digestive tract and long remission of a peptic ulcer that reduces probability of such complications as bleedings, also effectively, as well as a constant maintenance therapy.
Other effects connected with inhibition of secretion of hydrochloric acid
At the patients accepting the drugs lowering secretion of glands of a stomach during a long period formation of ferruterous cysts in a stomach is more often noted; cysts high-quality also pass independently against the background of therapy continuation. These phenomena are caused by physiological changes in result of inhibition of secretion of hydrochloric acid.
Decrease in secretion of hydrochloric acid in a stomach under the influence of inhibitors of the proton pump or other means reducing acidity of a stomach, leads to increase in growth of normal intestinal microflora that in turn can lead to insignificant increase in risk of development of the intestinal infections caused by bacteria of the sort Salmonella spp. and Campylobacter spp., and at the hospitalized patients probably also Clostridium difficile bacterium.
During treatment by the drugs lowering secretion of glands of a stomach, concentration of gastrin in blood serum increases. Owing to decrease in secretion of hydrochloric acid concentration of chromogranin A (CgA) increases. Increase in concentration of CgA can exert impact on results of inspections for detection of neuroendocrinal tumors. For prevention of this influence therapy by inhibitors of the proton pump needs to be suspended in 5-14 days prior to carrying out a research of concentration of CgA. If during this time concentration of CgA did not return to normal value, the research should be repeated.
At children and adult patients, it is long accepting омепразол, increase in quantity of enterokhromaffinopodobny cells probably connected with increase in concentration of gastrin in blood serum was noted. This phenomenon has no clinical importance.

Pharmacokinetics. Distribution
Omeprazol is absorbed in a small bowel, usually within 3-6 hours. Bioavailability after intake makes about 60%. Meal does not influence bioavailability of an omeprazol.
The indicator of a svyazyvayemost of an omeprazol with proteins of plasma makes about 95%, the volume of distribution makes 0,3 l/kg.
Metabolism
Omeprazol is completely metabolized in a liver. The main enzymes participating in process of metabolism, CYP2C19 and CYP3A4. The formed metabolites – sulphone, sulfide and hydroxy-omeprazol do not exert considerable impact on secretion of hydrochloric acid.
The general plasma clearance makes 0,3-0,6 l/min. Bioavailability of an omeprazol increases approximately by 50% at repeated reception in comparison with reception of a single dose.
Excretion
The elimination half-life makes about 40 minutes (30 - 90 minutes). About 80% are removed in the form of metabolites by kidneys, and other part – intestines.
Special groups of patients
Considerable changes of bioavailability of an omeprazol at elderly patients or at patients with an impaired renal function are noted. At patients with the broken function of a liver increase in bioavailability of an omeprazol and considerable reduction of plasma clearance is noted.

Indications to use:

Лосек® MАПС® is intended for treatment of the following diseases:
- duodenum ulcer
- stomach ulcer
- NPVP the associated ulcers and erosion of a stomach and a duodenum
- Helicobacter pylori eradikation at a peptic ulcer
- reflux esophagitis
- symptomatic gastroesophageal reflux disease
- the dyspepsia connected with a hyperoxemia
- Zollingera-Ellison's syndrome.

Route of administration and doses:

Inside. The pill Losek® MАПС® is recommended to be taken in the morning, it is necessary to swallow of a tablet entirely, washing down with liquid. Tablets cannot be chewed or split up.
Tablets can be dissolved in water or slightly acidified liquid, for example, in fruit juice. The received solution has to be used within 30 min. To be sure of reception of a full dose, pour in a glass liquid half again, shake up and drink.
Duodenum ulcer.
Patients with an active ulcer of a duodenum are recommended to accept Losek® of MАПС® 20 mg of 1 times a day. Drug provides bystry elimination of symptoms. At most of patients healing of an ulcer occurs within 2 weeks. When within 2 weeks full healing of an ulcer does not occur, healing is reached at the subsequent 2-week administration of drug of Losek® of MАПС®.
To patients with an ulcer of a duodenum a little susceptible to treatment, usually appoint Losek® of MАПС® 40 mg of 1 times a day; healing of an ulcer usually occurs within 4 weeks.
For prevention of a recurrence recommend to patients with an ulcer of a duodenum Losek® of MАПС® 10 mg of 1 times a day. In case of need it is possible to increase a dose to 20-40 mg of 1 times a day.
Stomach ulcer.
The recommended dose – Losek® of MАПС® 20 mg of 1 times a day. Drug provides bystry elimination of symptoms. At most of patients treatment comes within 4 weeks. When after the first course of administration of drug full healing does not occur, usually appoint a repeated 4 weeks course of treatment during which healing is reached.
To patients with the stomach ulcer a little susceptible to treatment, usually appoint Losek® of MАПС® 40 mg of 1 times a day; healing is usually reached within 8 weeks.
For prevention of a recurrence recommend to patients with stomach ulcer Losek® of MАПС® 20 mg of 1 times a day. In case of need it is possible to increase a dose to 40 mg of 1 times a day.
NPVP the associated ulcers and erosion of a stomach and a duodenum
In the presence of NPVP of the associated stomach ulcers, a duodenum or gastroduodenal erosion at patients with the stopped or continuing therapy of NPVP the recommended dose of the drug Losek® MАПС® – 20 mg of 1 times a day. Drug provides bystry elimination of symptoms, at most of patients treatment comes within 4 weeks. At those patients who had no izlechivaniye during the period of initial therapy healing is usually reached at repeated 4-week administration of drug.
For the prevention of ulcers and erosion of a stomach and a duodenum and symptoms of dyspepsia connected with reception of NPVP the dose of the drug Losek® MАПС® – 20 mg of 1 times a day is recommended.
The modes of an eradikation Helicobacter pylori (Hp) at a peptic ulcer.
Ternary scheme of treatment:
Лосек® MАПС® 20 mg, amoxicillin of 1 g and кларитромицин 500 mg. To accept all drugs 2 times a day within one week
or Losek® of MАПС® 20 mg, metronidazole of 400 mg (or Tinidazolum of 500 mg) and кларитромицин 250 mg. To accept all drugs 2 times a day within one week
or
Лосек® MАПС® 40 mg of 1 times a day, and also amoxicillin of 500 mg and metronidazole of 400 mg 3 times a day within one week.
Two-component scheme of treatment:
Лосек® MАПС® 40 - 80 mg daily and amoxicillin of 1,5 g daily (the dose should be divided into parts) within two weeks. During clinical tests 3 times a day within two weeks applied amoxicillin in a daily dose of 1,5-3 g, Losek® of MАПС® 40 mg of 1 times a day and кларитромицин 500 mg.
For ensuring full healing to carry out further treatment according to recommendations in the sections "Duodenum Ulcer" and "Stomach ulcer".
When after passing of a course of treatment test on Helicobacter pylori remains positive, the course of treatment can be repeated.
Reflux esophagitis.
The recommended dose – on one tablet Losek® MАПС® 20 of mg of 1 times a day. Drug provides bystry elimination of symptoms. At most of patients treatment comes within 4 weeks. When after the first course of administration of drug full treatment does not come, usually appoint a repeated 4 weeks course of treatment during which treatment is reached.
To patients with a severe form the reflux of an esophagitis is recommended to Losek® of MАПС® 40 mg of 1 times a day; treatment usually comes within 8 weeks.
To patients about a reflux esophagitis in a stage of remission appoint Losek® of MАПС® 10 mg of 1 times a day in the form of long courses of a maintenance therapy. In case of need it is possible to increase a dose to 20-40 mg.
Symptomatic gastroesophageal reflux disease.
The recommended dose – Losek® of MАПС® 20 mg of 1 times a day. Drug provides bystry elimination of symptoms. The therapeutic effect can be reached at a daily dose of 10 mg therefore individual selection of a dose is not excluded. If after 4 weeks of treatment (Losek® of MАПС® 20 mg of 1 times a day) symptoms do not disappear, additional inspection of the patient is recommended.
The dyspepsia connected with a hyperoxemia.
For simplification of pains and/or elimination of sensations of discomfort in epigastric area, with heartburn or without heartburn, appoint Losek® of MАПС® 20 mg of 1 times a day. The therapeutic effect can be reached at a dose of 10 mg of 1 times a day therefore treatment can be begun with this dose. If after 4 weeks of treatment (Losek® of MАПС® 20 mg of 1 times a day) symptoms do not disappear, additional inspection of the patient is recommended.
Zollingera-Ellison's syndrome.
To patients with Zollingera-Ellison's syndrome drug is appointed in an individual dosage. Treatment is continued according to clinical indications so long as far as it is necessary. The recommended initial dose – Losek® of MАПС® 60 mg daily. All patients with a severe form have diseases and also when other therapeutic methods did not result in desirable result, more than 90% of patients had an effective use of drug at reception of 20-120 mg of Losek® of MАПС® daily. When the daily dose of drug exceeds 80 mg, the dose should be divided into two parts and to accept 2 times a day.
Renal failure.
For patients with a renal failure correction of a dose is not required.
Abnormal liver function.
At patients with an abnormal liver function bioavailability and an elimination half-life of an omeprazol from plasma increase. In this regard the dose of 10-20 mg a day is sufficient.
Patients of advanced age.
For patients of advanced age correction of a dose is not required.
Children.
Experience of use for children is limited.

Features of use:

In the presence of any alarming symptoms (for example, such as considerable spontaneous loss of body weight, repeated vomiting, a dysphagy, vomiting with impurity of blood or a melena), and also in the presence of stomach ulcer (or at suspicion of stomach ulcer) it is necessary to exclude existence of a malignant new growth as treatment by the drug Losek® MАПС® can lead to smoothing of symptomatology and delay diagnosis.
Combined use of an omeprazol with such drugs as атазанавир and нелфинавир is not recommended. By results of researches is noted pharmacokinetic / фармакодинамическое interaction between klopidogrely (a load dose of 300 mg and a maintenance dose of 75 mg/days) and omeprazoly (80 mg/days inside) which leads to decrease in exposure to an active metabolite of a klopidogrel on average for 46% and to decrease in the maximum inhibition ADF-indutsirovannoy in aggregation of thrombocytes on average by 16%. Therefore it is necessary to avoid simultaneous use of an omeprazol and a klopidogrel (see the section "Interaction with Other Medicines and Other Forms of Interaction").
Influence on ability to drive the car or other mechanisms
There are no data on influence of the drug Losek® MАПС® on ability to drive the car or other mechanisms. However, because during therapy can be observed dizziness, an illegibility of sight and drowsiness, it is necessary to be careful at control of motor transport or other mechanisms.

Side effects:

The side effects which are not depending on the mode of dosing of an omeprazol which were noted during clinical trials, and also at post-marketing use are included below.
Often
(> 1/100, <1/10)
Headache, abdominal pain, diarrhea, meteorism, nausea/vomiting, lock
Infrequently
(> 1/1000, <1/100)
Dermatitis, itch, rash, urticaria, drowsiness, sleeplessness, dizziness, paresthesias, indisposition, increase in activity of "hepatic" enzymes
Seldom
(> 1/10000, <1/1000)
Hypersensitivity reactions (for example, fever, a Quincke's disease, anaphylactic reaction / an acute anaphylaxis), a bronchospasm, hepatitis (with jaundice or without), a liver failure, encephalopathy at patients with liver diseases, an arthralgia, a mialgiya, muscular weakness, a leukopenia, thrombocytopenia, an agranulocytosis, a pancytopenia, a depression, a hyponatremia, excitement, aggression, confusion, hallucinations, taste disturbance, a sight illegibility, dryness in a mouth, stomatitis, digestive tract candidiasis, an alopecia, a photosensitization, a multiformny erythema, Stephens-Johnson's syndrome, a toxic epidermal necrolysis, intersticial nephrite, a gynecomastia, perspiration, peripheral hypostases, microscopic colitis
Very seldom
(<1/10000)
Hypomagnesiemia, hypocalcemia owing to a heavy hypomagnesiemia
It was reported about cases of formation of ferruterous cysts in a stomach at the patients accepting the drugs lowering secretion of glands of a stomach during a long period; cysts high-quality also pass independently against the background of therapy continuation.

Interaction with other medicines:

Influence of an omeprazol on pharmacokinetics of other medicines
Decrease in secretion of hydrochloric acid in a stomach at treatment omeprazoly and other inhibitors of the proton pump can lead to decrease or increase in absorption of other drugs which absorption depends on acidity of the environment.
Like other drugs reducing acidity of a gastric juice, treatment omeprazoly can lead to decrease in absorption of a ketokonazol, itrakonazol and erlotinib, and also to increase in absorption of such drugs as digoxin. Joint reception of an omeprazol in a dose of 20 mg and digoxin increases once a day bioavailability of digoxin for 10% (bioavailability of digoxin increased at a size up to 30% at 20% of patients).
It was shown what омепразол interacts with some anti-retrovirus drugs. Mechanisms and clinical value of these interactions are not always known. Increase in value рН against the background of therapy omeprazoly can influence absorption of anti-retrovirus drugs. Interaction at the level of CYP2C19 isoenzyme is also possible. At combined use of an omeprazol and some anti-retrovirus drugs, such as атазанавир and нелфинавир, against the background of therapy omeprazoly decrease in their concentration in serum is noted. In this regard combined use of an omeprazol with anti-retrovirus drugs, such as атазанавир and нелфинавир, it is not recommended.
At simultaneous use of an omeprazol and sakvinavir increase in concentration of a sakvinavir in serum was noted, at use with some other anti-retrovirus drugs their concentration did not change.
Omeprazol inhibits CYP2C19 – the main isoenzyme participating in his metabolism. Combined use of an omeprazol with other drugs in which metabolism CYP2C19 isoenzyme takes part such as diazepam, warfarin (R-warfarin) or other antagonists of vitamin K, Phenytoinum and цилостазол, can lead to delay of metabolism of these drugs. Observation of the patients accepting Phenytoinum and омепразол is recommended, Phenytoinum dose decline can be required. However the accompanying treatment omeprazoly in a daily dose of 20 mg does not influence concentration of Phenytoinum in a blood plasma at patients, is long accepting drug. At use of an omeprazol by the patients receiving warfarin or other antagonists of vitamin K monitoring of the international normalized relation is necessary; in some cases the dose decline of warfarin or other antagonist of vitamin K can be necessary. At the same time the accompanying treatment omeprazoly in a daily dose of 20 mg does not lead to change of time of coagulation at patients, is long accepting warfarin.
Use of an omeprazol in a dose of 40 mg led to increase in Cmax and AUC of a tsilostazol by 18% and 26%, respectively once a day; for one of active metabolites of a tsilostazol increase made 29% and 69%, respectively. By results of researches it is noted pharmacokinetic / фармакодинамическое interaction between klopidogrely (a load dose of 300 mg and a maintenance dose of 75 mg/days) and omeprazoly (80 mg/days inside) which leads to decrease in exposure to an active metabolite of a klopidogrel, on average, for 46% and to decrease in the maximum inhibition ADF-indutsirovannoy in aggregation of thrombocytes, on average, for 16%. The clinical importance of this interaction is not clear. Increase in risk of cardiovascular complications at combined use of a klopidogrel and inhibitors of the proton pump, including an omeprazol, was not shown in a prospective randomized incomplete research with participation more than 3760 patients receiving placebo or омепразол in a dose of 20 mg/days along with therapy klopidogrely and acetylsalicylic acid (ASK), and more than 47000 patients are not confirmed with the additional nonrandomized analysis of clinical outcomes of large-scale prospective randomized researches with participation. Results of a number of the observation researches are contradictory and do not give definite answer about existence or lack of the increased risk of tromboembolic cardiovascular episodes against the background of combined use of a klopidogrel and inhibitors of the proton pump. At use of a klopidogrel together with the fixed combination of 20 mg of esomeprazole and 81 mg of ASK exposure to an active metabolite of a klopidogrel decreased almost by 40% in comparison with monotherapy klopidogrely, at the same time the maximum levels of inhibition ADF-indutsirovannoy of aggregation of thrombocytes were identical that is probably connected with a concomitant use of ASK in a low dose.
Omeprazol does not influence metabolism of drugs, metaboliziruyemy an isoenzyme of CYP3A4, such as, cyclosporine, lidocaine, quinidine, oestradiol, erythromycin and будесонид.
Interaction of an omeprazol with the following drugs is not revealed: caffeine, theophylline, S-warfarin, piroxicam, diclofenac, Naproxenum, метопролол, propranolol and ethanol.
At simultaneous use of an omeprazol and takrolimus increase in concentration of a takrolimus in blood serum was noted.
At some patients noted increase in concentration of a methotrexate against the background of combined use with inhibitors of the proton pump. At purpose of high doses of a methotrexate it is necessary to consider the possibility of temporary cancellation of an omeprazol.
Influence of medicines on pharmacokinetics of an omeprazol
Isoenzymes of CYP2C19 and CYP3A4 participate in metabolism of an omeprazol. Combined use of an omeprazol and inhibitors of isoenzymes of CYP2C19 and CYP3A4, such as кларитромицин and вориконазол, can lead to increase in concentration of an omeprazol in a blood plasma due to delay of metabolism of an omeprazol. Combined use of a vorikonazol and omeprazol leads to more than double increase in AUC of an omeprazol. Due to the good tolerance of high doses of an omeprazol, at short combined use of the specified drugs dose adjustment of an omeprazol is not required.
The medicines inducing isoenzymes of CYP2C19 and CYP3A4 which such as rifampicin and drugs of a St. John's Wort is made a hole at combined use with omeprazoly can lead to decrease in concentration of an omeprazol in a blood plasma due to acceleration of metabolism of an omeprazol.

Contraindications:

The known hypersensitivity to an omeprazol, the replaced benzimidazoles or other ingredients which are a part of drug.

With care
In the presence of such symptoms as considerable spontaneous loss in weight, frequent vomiting, a dysphagy, vomiting with blood or a melena, and also in the presence of stomach ulcer (or suspicion of stomach ulcer) it is necessary to exclude existence of a malignant new growth as treatment can lead to masking of symptoms and, thus, detain diagnosis.
Use during pregnancy and breastfeeding
Results of researches showed lack of side effect of an omeprazol on health of pregnant women, on a fruit or on the newborn.
Лосек® MАПС® can be applied during pregnancy.
Omeprazol gets into breast milk, however at its use in therapeutic doses of impact on the child it is improbable.

Overdose:

Single peroral doses of the drug Losek® MАПС® to 400 mg did not cause any heavy symptoms. At reception of adult 560 mg of an omeprazol moderate intoxication was noted. At increase in a dose the speed of elimination of drug did not change (kinetics of the first order), specific treatment at the same time was not required.
Symptoms: dizziness, confusion of consciousness, apathy, headache, dilatation of vessels, tachycardia, nausea, vomiting, meteorism, diarrhea.
Treatment: symptomatic treatment, if necessary gastric lavage, purpose of absorbent carbon.

Storage conditions:

Period of validity 3 years. Not to apply after the period of validity specified on packaging. To store at a temperature not above 25 °C. After use it is dense to close a cover of a bottle. To store in the places unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated 10 mg or 20 mg.
On 14 tablets in a plastic bottle with the screwing-up plastic cover with control of the first opening. Each bottle is packed into a cardboard pack with the application instruction.