Universal reference book for medicines
Product name: LOSEK ® MAPS ® (LOSEC MUPS)

Active substance: omeprazole

Type: H + -K + -ATPase inhibitor.
Antiulcer drug
Manufacturer: ASTRAZENECA UK (UK) manufactured by ASTRAZENECA (Sweden)
Composition, form of production and packaging
The tablets covered with a film cover of
light pink color, oblong, biconcave, with an engraving "10 mG" on one side and a badge on the other.

1 tab.

omeprazole magnesium 10.3 mg,

which corresponds to the content of omeprazole 10 mg

Auxiliary substances: microcrystalline cellulose - 170 mg, glyceryl monostearate (40-55) 1.1 mg, giprolose 3.5 mg, hypromellose 10 mg, magnesium stearate 0.5 mg, methacrylic acid and ethacrylic acid copolymer 23 mg, paraffin 0.1 mg, macrogol 1.9 mg, polysorbate 80 0.1 mg, crospovidone 3.5 mg, sodium stearyl fumarate 0.3 mg, sucrose spherical granules 22 mg, talc 6.1 mg, titanium dioxide (E171) 1.8 mg, triethyl citrate 6.8 mg, iron dye oxide red (E172) - 0.04 mg, iron dye oxide yellow (E172) - 0.02 mg.

14 pcs.
- plastic bottles (1) - packs of cardboard.
The tablets covered with a film cover of pink color, oblong, biconcave, with engraving "20 mG" on one side and a badge on the other.

1 tab.

omeprazole magnesium 20.6 mg,

which corresponds to the content of omeprazole 20 mg

Auxiliary substances: microcrystalline cellulose - 220 mg, glyceryl monostearate (40-55) - 1.4 mg, giprolose - 4.8 mg, hypromellose - 15 mg, magnesium stearate - 0.7 mg, methacrylic and ethacrylic acid copolymer - 27 mg, paraffin 0.2 mg, macrogol 2.5 mg, polysorbate 80 0.1 mg, crospovidone 4.6 mg, sodium stearyl 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 oxide red (E172) 0.03 mg.

14 pcs.
- plastic bottles (1) - packs of cardboard.
28 pcs.
- plastic bottles (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2013.

PHARMACHOLOGIC EFFECT

Mechanism of action

Omeprazole is a weak base.
Concentrates in the acidic environment of the secretory tubules of parietal cells of the gastric mucosa, is activated and inhibits the proton pump - the enzyme H + , K + -ATPase. Effect of omeprazole on the last stage of the process of formation of hydrochloric acid in the stomach is dose-dependent and provides a highly effective inhibition of basal and stimulated secretion of hydrochloric acid regardless of the stimulating factor.
Effect on secretion of gastric juice

Losek ® MAPS ® with daily oral administration provides fast 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 Losek ® MAPS ® 20 mg causes a steady decrease in 24-hour gastric acidity by at least 80%. At the same time, the average maximum concentration of hydrochloric acid is reduced after pentagastrin stimulation by 70% within 24 hours.
In patients with duodenal ulcer Losek ® MAPS ® 20 mg with daily oral administration maintains the acidity value at pH> 3 on average for 17 hours per day in the intragastric environment.

Inhibition of hydrochloric acid secretion depends on the area under the concentration-time curve (AUC) of omeprazole, and not on the concentration of the drug in the plasma at a given time.

Action on Helicobacter pylori

Omeprazole has a bactericidal effect on Helicobacter pylori in vitro.
Helicobacter pylori eradication with omeprazole combined with antibacterial agents is accompanied by rapid elimination of symptoms, high healing of gastrointestinal mucosal defects and prolonged remission of peptic ulcer, which reduces the likelihood of complications such as bleeding as effectively as constant maintenance therapy.
Other effects associated with inhibition of hydrochloric acid secretion

In patients taking drugs that reduce the secretion of the glands of the stomach, for a long period of time, the formation of glandular cysts in the stomach is more often noted;
cysts are benign and pass independently on the background of continuation of therapy. These phenomena are caused by physiological changes due to inhibition of hydrochloric acid secretion.
The decrease in the secretion of hydrochloric acid in the stomach under the influence of proton pump inhibitors or other gastric acid-lowering agents, leads to an increase in the growth of normal intestinal microflora, which in turn can lead to a slight increase in the risk of intestinal infections caused by the bacteria of the genus Salmonella spp.
and Campylobacter spp., and in hospitalized patients, probably also the bacterium Clostridium difficile.
During treatment with drugs that reduce the secretion of the glands of the stomach, the concentration of gastrin in the blood serum

increases.
Due to a decrease in the secretion of hydrochloric acid, the concentration of chromogranin A (CgA) increases. An increase in CgA concentration may influence the results of the examinations to identify neuroendocrine tumors. For
To prevent this effect, therapy with proton pump inhibitors should be stopped 5 to 14 days before the CgA concentration test.
If during this time the concentration of CgA did not return to the normal value,
the study should be repeated.

In children and adult patients who took omeprazole for a long time, there was an increase in the number of enterochromaffin-like cells, probably due to an increase in the concentration of gastrin in the blood serum.
Clinical significance of this phenomenon is not.
PHARMACOKINETICS

Distribution

Omeprazole is absorbed in the small intestine, usually for 3-6 hours.
Bioavailability after oral administration is approximately 60%. Eating does not affect the bioavailability of omeprazole.
The binding index 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% with repeated admission as compared with single dose administration.
Excretion

T 1/2 is about 40 minutes (30-90 minutes).
About 80% is excreted as metabolites by the kidneys, and the rest by the intestine.
Special patient groups

There were no significant changes in the bioavailability of omeprazole in elderly patients or in patients with impaired renal function.

In patients with impaired liver function, there is an increase in the bioavailability of omeprazole and a significant decrease in plasma clearance.

INDICATIONS

Losek ® MAPS ® is designed to treat the following diseases:

- duodenal ulcer;

- stomach ulcer;

- NSAID associated ulcers and erosions of the stomach and duodenum;

- eradication of Helicobacter pylori with peptic ulcer;

- reflux esophagitis;

- symptomatic gastro-oesophageal reflux disease;

- dyspepsia associated with increased acidity;

- Zollinger-Ellison syndrome.

DOSING MODE

Inside.
Tablets Losek ® MAPS ® is recommended to be taken in the morning, the tablet should be swallowed whole, washed down with 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 the liquid back into the glass halfway, shake and drink.
Duodenal ulcer

Patients with an active duodenal ulcer are recommended to take Losek ® MAPS ® 20 mg once a day.
The drug provides a rapid elimination of symptoms. In most patients, healing of the ulcer occurs within 2 weeks. In those cases when complete healing of the ulcer does not occur within 2 weeks, the healing is achieved with the subsequent 2-week administration of Losek ® MAPS ® .
Patients with an ulcer of the duodenum, little susceptible to treatment, are usually prescribed Losek ® MAPS ® 40 mg once a day;
healing of the ulcer usually occurs within 4 weeks.
To prevent relapse, patients with a duodenal ulcer are recommended Losek ® MAPS ® 10 mg once a day.
If necessary, the dose can be increased to 20-40 mg once a day.
Stomach ulcer

The recommended dose is Losek ® MAPS ® 20 mg once a day.
The drug provides a rapid elimination of symptoms. In most patients, the cure comes within 4 weeks. In those cases when after the first course of taking the drug complete healing does not occur, usually a repeated 4-week course of treatment, during which healing is achieved.
Patients with a stomach ulcer that is less susceptible to treatment are usually prescribed Losek ® MAPS ® 40 mg once a day;
healing is usually achieved within 8 weeks.
To prevent relapse, patients with stomach ulcers are recommended Losek ® MAPS ® 20 mg once a day.
If necessary, the dose can be increased to 40 mg once a day.
NSAID associated ulcers and erosion of the stomach and duodenum

In the presence of NSAIDs associated gastric ulcers, duodenal ulcers or gastroduodenal erosions in patients with discontinued or continuing therapy with NSAIDs, the recommended dose of Losek ® MAPS ® is 20 mg once daily.
The drug provides a rapid elimination of symptoms, the majority of patients cure occurs within 4 weeks. In those patients who have not had a cure during the initial therapy period, healing is usually achieved with a repeated 4-week treatment.
For the prevention of ulcers and erosions of the stomach and duodenum and symptoms of dyspepsia associated with the administration of NSAIDs, a dose of Losek ®MAPS ® 20 mg once daily is recommended.

Modes of eradication Helicobacter pylori with peptic ulcer.

Three-component treatment regimen:

Losek ® MAPS ® 20 mg, amoxicillin 1 g and clarithromycin 500 mg.
All drugs take 2 times a day for one week
or

Losek ® MAPS ® 20 mg, metronidazole 400 mg (or tinidazole 500 mg) and clarithromycin 250 mg.
All drugs take 2 times a day for one week
or

Losek ® MAPS ® 40 mg once a day, as well as amoxicillin 500 mg and metronidazole 400 mg 3 times daily for one week.

Two-component treatment regimen:

Losek ® MAPS ® 40-80 mg daily and amoxicillin 1.5 g daily (dose should be divided into parts) within two weeks.
During clinical trials, amoxicillin was used at a daily dose of 1.5-3 g, Losek® MAPS® 40 mg once daily and
clarithromycin 500 mg 3 times a day for two weeks.

To ensure complete healing, further treatment should be carried out in accordance with the recommendations in the sections "Duodenal ulcer" and "Gastric ulcer."

In those cases when after the course of treatment the test for Helicobacter pylori remains positive, the course of treatment can be repeated.

Reflux esophagitis

The recommended dose is one Losek ® MAPS ® 20 mg tablet once a day.
The drug provides a rapid elimination of symptoms. In most patients, the cure comes within 4 weeks. In those cases when, after the first course of taking the drug, there is no complete cure, usually a repeated 4-week course of treatment is prescribed, in
during which a cure is achieved.

Patients with severe form of esophagitis reflux are recommended Losek ® MAPS ® 40 mg once a day;
Cure usually occurs within 8 weeks.
Patients with reflux-esophagitis in remission are prescribed Losek ® MAPS ® 10 mg once a day in the form of long courses of maintenance therapy.
If necessary, the dose can be increased to 20-40 mg.
Symptomatic gastro-oesophageal reflux disease .

The recommended dose is Losek ® MAPS ® 20 mg once a day.
The drug provides a rapid elimination of symptoms. The therapeutic effect can be achieved with a daily dose of 10 mg, so individual dose selection is not excluded. If after 4 weeks of treatment (Losek ® MAPS ® 20 mg once a day) the symptoms do not disappear, an additional examination of the patient is recommended.
Dyspepsia associated with increased acidity

To alleviate pain and / or eliminate discomfort in the epigastric region, with heartburn or without heartburn, Losek ® MAPS ® 20 mg once a day is prescribed.
The therapeutic effect can be achieved at 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 once a day) the symptoms do not disappear, an additional examination of the patient is recommended.
Zollinger-Ellison Syndrome

Patients with Zollinger-Ellison syndrome the drug is prescribed in an individual dosage.
Treatment is continued according to clinical indications as long as necessary.The recommended initial dose is Losek ® MAPS ® 60 mg daily. In all patients with severe disease, and when other therapeutic methods did not lead to the desired result, the drug was effective in more than 90% of patients receiving 20-120 mg Losek ® MAPS ® daily. In those cases when 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 the half-life of omeprazole plasma 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

Experience with children is limited.

SIDE EFFECT

Below are the side effects,
independent of the dosing regimen of omeprazole, which were noted during clinical trials, as well as in post-marketing applications.
Often (> 1/100, <1/10) Headache, abdominal pain, diarrhea, flatulence, nausea / vomiting, constipation

Infrequent (> 1/1000, <1/100) Dermatitis, pruritus, rash, urticaria, drowsiness, insomnia, dizziness, paresthesia, malaise, increased activity of hepatic enzymes

Rarely (> 1/10000, <1/1000) Hypersensitivity reactions (eg, fever, angioedema, anaphylactic reaction / anaphylactic shock), bronchospasm, hepatitis (with or without jaundice), liver failure, encephalopathy in patients with liver disease, arthralgia , myalgia, muscle weakness, leukopenia, thrombocytopenia, agranulocytosis, pancytopenia, depression, hyponatremia, agitation, aggression, confusion, hallucinations, impaired taste, blurred vision, dry mouth, stomatitis, candidiasis GI tract, alopecia, photosensitizer
I, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, interstitial nephritis, gynecomastia, sweating, peripheral edema, microscopic colitis
Very rarely (<1/10000) Hypomagnesemia, hypocalcemia due to severe hypomagnesemia, hypokalemia due to hypomagnesemia

There have been reports of cases of the formation of glandular cysts in the stomach in patients taking drugs that lower

secretion of the glands of the stomach, for a long period of time;
cysts are benign and pass independently on the background of continuation of therapy.
CONTRAINDICATIONS

- a known hypersensitivity to omeprazole, substituted benzimidazoles or other ingredients that make up the drug.

Carefully

If there are symptoms such as significant spontaneous weight loss, frequent vomiting, dysphagia, vomiting with blood or melena, and if there is a stomach ulcer (or suspected gastric ulcer), the presence of a malignant tumor should be excluded, since treatment can lead to masking of symptoms and , thus delaying the diagnosis.

PREGNANCY AND LACTATION

The results of the studies showed no side effects of omeprazole on the health of pregnant women, on the fetus or on the newborn.
Losek ® MAPS ® can be used during pregnancy.
Omeprazole penetrates into breast milk, but when applied in therapeutic doses, exposure to the baby is unlikely.

APPLICATION FOR FUNCTIONS OF THE LIVER

For patients with impaired renal function, dose adjustment is not required.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

In patients with impaired liver function, bioavailability and the half-life of omeprazole plasma increase.
In this regard, a dose of 10-20 mg per day is sufficient.
APPLICATION FOR CHILDREN

Experience with children is limited.

APPLICATION IN ELDERLY PATIENTS

For elderly patients, dose adjustment is not required.

SPECIAL INSTRUCTIONS

In the presence of any anxiety symptoms (for example, such as significant spontaneous weight loss,
repeated
vomiting, dysphagia, vomiting with an admixture of blood or melena), as well as in the presence of a stomach ulcer (or with suspected ulcer

stomach), the presence of malignant neoplasm should be excluded, since treatment with Losek® MAPS® can lead to a smoothing of the symptoms
and to postpone the diagnosis.
It is not recommended the joint use of omeprazole with such drugs as atazanavir and nelfinavir.

Based on the results of the studies,
pharmacokinetic / pharmacodynamic interaction between clopidogrel (loading dose 300 mg and maintenance dose 75 mg / day) and omeprazole (80 mg / day inwards), which leads to a decrease Exposure to the active metabolite of clopidogrel averaged 46% and a decrease in the maximum inhibition of ADP-induced platelet aggregation by an average of 16%. Therefore, simultaneous use of omeprazole and clopidogrel should be avoided.
Individual observational studies suggest that treatment with proton pump inhibitors may slightly increase the risk of osteoporosis-related fractures, but not observed in other studies of similar increased risk.
In a randomized, double-blind, controlled clinical studies of omeprazole and esomeprazole, including two open-label studies with a duration of treatment for more than 12 years, the relationship osteoporotic fractures has not been confirmed with the use of proton pump inhibitors.
Although a causal relationship omeprazole / esomeprazole with fractures to osteoporosis has not been established, patients with a risk of osteoporosis or fractures on his background should be kept under appropriate clinical supervision.
The effect on the ability to drive or other mechanisms
are no data on the influence of drug Losek ® CI ® driving ability or other mechanisms. However, due to the fact that during therapy may experience dizziness, blurred vision and drowsiness, use caution when driving or operating other machinery.
OVERDOSE

A single oral dose of the drug Losek ® CI ® 400 mg did not cause any severe symptoms. When receiving the 560 mg of omeprazole adults had moderate toxicity. When increasing the dose rate of elimination did not change (first order kinetics), specific treatment is not required.
Symptoms: dizziness, confusion, lethargy, headache, dilation of blood vessels, tachycardia, nausea, vomiting, flatulence, diarrhea.
Treatment: symptomatic treatment, if necessary - gastric lavage, appointment of activated carbon.
DRUG INTERACTION

Effect of omeprazole on the pharmacokinetics of other drugs
Reduced secretion of hydrochloric acid in the stomach in the treatment of omeprazole and other proton pump inhibitors can cause a reduction or increase the absorption of other drugs, the absorption of which depends on the acidity of the medium.
Like other drugs, lowering gastric acidity, omeprazole treatment may result in decreased absorption of ketoconazole, itraconazole and erlotinib, as well as improving the suction of drugs such as digoxin.
Co-administration of omeprazole 20 mg once daily and digoxin increases the bioavailability of digoxin in 10%
(bioavailability of digoxin was increased by up to 30% in 20% of patients).
It has been shown that omeprazole interact with some antiretroviral drugs.
Mechanisms and clinical implications of these interactions are not always known. The increase in pH during treatment with omeprazole may interfere with the absorption of antiretroviral drugs. It is also possible for the interaction CYP2C19 isozyme level. If concomitant use of omeprazole and certain antiretroviral drugs such as atazanavir and nelfinavir, against the background of omeprazole therapy, there is a decrease in their serum concentrations. Therefore, the combined use of omeprazole with antiretroviral drugs, such as atazanavir and nelfinavir is not recommended.
With simultaneous use of omeprazole saquinavir and saquinavir increase was observed in serum, when used with some other antiretroviral drugs, their concentration was not changed.
Omeprazole inhibits CYP2C19 - basic isozyme involved in its metabolism. The combined use of omeprazole with other drugs in metabolism which participates isozyme CYP2C19, 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 to monitor the patients receiving phenytoin and omeprazole, may require dose reduction of phenytoin. However, co-treatment with omeprazole in a daily dose of 20 mg did not affect the concentration of phenytoin in blood plasma of patients receiving long-term medication. When omeprazole patients receiving warfarin and other vitamin K antagonists, requires monitoring of international normalized ratio;in some cases you may need a dose reduction of warfarin or other vitamin K antagonists However concomitant treatment with omeprazole 20 mg daily does not change coagulation time in patients receiving long-term warfarin.
Omeprazole 40mg once a day resulted in an increase in C max and AUC cilostazol by 18% and 26%, respectively; for one of the active metabolites cilostazol increase was 29% and 69%, respectively. According to the research mentioned pharmacokinetic / pharmacodynamic interaction between clopidogrel (loading dose of 300 mg, and the maintenance dose of 75 mg / day) and omeprazole (80 mg / day orally), which leads to lower exposure to the active metabolite of clopidogrel, on average, by 46% and decrease maximal inhibition of ADP-induced platelet aggregation, on average, 16%.
The clinical significance of this interaction is not clear. Increased risk of cardiovascular complications in
combined use of clopidogrel and proton pump inhibitors, including omeprazole, have not been shown in
prospective randomized incomplete study involving more than 3760 patients receiving placebo or omeprazole 20 mg / day concurrently with therapy with clopidogrel and acetylsalicylic acid (ASA), and
confirmed by additional analysis of non-randomized clinical outcomes of large-scale, prospective, randomized studies involving more than 47,000 patients.
A number of observational studies are inconsistent and do not give a clear answer about the presence or
absence of an increased risk of thromboembolic cardiovascular events against the background of the joint use of clopidogrel and proton pump inhibitors.
When clopidogrel together with a fixed combination of 20 mg of esomeprazole and 81 mg ASA exposure to the
active metabolite of clopidogrel decreased by almost 40% compared to a monotherapy clopidogrel, with
maximal levels of inhibition of ADP-induced platelet aggregation were identical, which is probably due to the simultaneous receiving a low dose of ASA.
Omeprazole does not affect the metabolism of drugs metabolized isoenzyme CYP3A4, such as cyclosporin, lidocaine, quinidine, estradiol, erythromycin and budesonide.
Not revealed the interaction of omeprazole with the following medications: caffeine, theophylline, S -varfarin, piroxicam, diclofenac, naproxen, metoprolol, propranolol and ethanol.
With simultaneous use of omeprazole and tacrolimus was observed increase of tacrolimus concentrations in blood serum.
Some patients noted increased concentration of methotrexate in the background of the joint use with proton pump inhibitors. When high doses of methotrexate should be considered a temporary cancellation of omeprazole.
Effect of drugs on the pharmacokinetics of omeprazole
The metabolism of omeprazole involving isozymes SYP2C19 and SYP3 A4. The combined use of omeprazole and inhibitors izofermentoz SYP2C19 and CYP3A4, such as clarithromycin and voriconazole, can lead to increased concentration of omeprazole in blood plasma by slowing down the metabolism of omeprazole. The combined use of voriconazole and omeprazole results in a more than twofold increase in AUC of omeprazole. Due to good tolerability of high-dose omeprazole after brief joint application of these drugs is not required omeprazole dose correction.
Medications which induce isozymes CYP2C19 and CYP3A4, such as rifampicin and preparations Hypericum perforatum, or combined with omepraeolom may lead to a decrease in the concentration of omeprazole in blood plasma by accelerating the metabolism of omeprazole.
TERMS OF RELEASE FROM PHARMACY

On prescription.

TERMS AND CONDITIONS OF STORAGE

Store at a temperature not exceeding 25 ° C.
After application of the vial cap tightly. Keep out of the reach of children. Shelf life - 3 years.
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