Losek - instructions for use, reviews, analogs and formulations (tablets 10 mg and 20 mg MAP) of a drug for the treatment of stomach ulcers and duodenal ulcers, gastritis, esophagitis in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Losek. Comments of visitors of the site - consumers of this medication, as well as opinions of doctors specialists on the use of Losek in their practice are presented. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues Losek in the presence of existing structural analogs. Use for treatment of stomach ulcers and duodenal ulcers, gastritis, esophagitis in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Losek - inhibits the last stage of the formation of hydrochloric acid, inhibits basal and stimulated (regardless of the type of inducer) secretion of hydrochloric acid.

Omeprazole (the active substance of the drug Losek) 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. 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.

Losek with daily oral administration provides a 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 ulcers, Losek Maps 20 mg with daily oral administration maintains an acidity value in the intragastric environment at a pH greater than 3 on average for 17 hours per day.

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 (Helicobacter)

Omeprazole has a bactericidal effect on Helicobacter pylori. 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.

Decrease in 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. (salmonella) 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. 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.

Composition

Omeprazole magnesium + auxiliary substances.

Pharmacokinetics

Losek absorbed in the small intestine, usually for 3-6 hours. Bioavailability after ingestion 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. 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 significantly affect the secretion of hydrochloric acid. The bioavailability of omeprazole increases by approximately 50% with repeated admission as compared with single dose administration. About 80% is excreted as metabolites by the kidneys, and the rest by the intestine.

Indications

duodenal ulcer;
stomach ulcer;
NSAIDs associated ulcers and erosion of the stomach and duodenum;
eradication of Helicobacter pylori in peptic ulcer;
reflux esophagitis;
symptomatic gastroesophageal reflux disease;
dyspepsia associated with increased acidity;
Zollinger-Ellison syndrome.

Forms of release

Tablets coated with 10 mg and 20 mg Losek Maps (sometimes mistakenly called capsules).

Instructions for use and reception schemes

Inside. Losek Maps pills are recommended 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 ulcer of the duodenum are advised 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 the healing of the ulcer does not occur within 2 weeks, healing is achieved with a subsequent 2-week treatment with Losek Mups.

Patients with a duodenal ulcer, a 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, not very 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 a stomach ulcer 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 ongoing therapy with NSAIDs, the recommended dose of Losek Maps is 20 mg once daily. The drug provides a rapid elimination of symptoms, in most 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.

To prevent ulcers and erosions of the stomach and duodenum, as well as the symptoms of dyspepsia associated with taking non-steroidal anti-inflammatory drugs (NSAIDs), a dose of Losek Maps 20 mg once daily is recommended.

Modes of eradication of Helicobacter pylori in peptic ulcer disease

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

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

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

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 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, during which cure is achieved, is prescribed.

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-term courses of maintenance therapy. If necessary, the dose can be increased to 20-40 mg.

Symptomatic gastroesophageal 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 relieve 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 also 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 of 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.

Side effect

headache;
abdominal pain;
diarrhea, constipation;
flatulence;
nausea, vomiting;
dermatitis;
itching;
rash;
hives;
drowsiness;
insomnia;
dizziness;
paresthesia;
malaise;
increased activity of hepatic enzymes;
hypersensitivity reactions (eg, fever, angioedema, anaphylactic reaction, or anaphylactic shock);
bronchospasm;
hepatitis (with jaundice or without);
liver failure;
encephalopathy in patients with liver disease;
arthralgia;
myalgia;
muscle weakness;
leukopenia, thrombocytopenia, agranulocytosis, pancytopenia;
depression;
hyponatremia;
excitation;
aggression;
confusion;
hallucinations;
a taste disorder;
blurred vision;
dry mouth;
stomatitis;
Candidiasis of the gastrointestinal tract;
alopecia;
photosensitization;
erythema multiforme;
Stevens-Johnson syndrome;
toxic epidermal necrolysis;
interstitial nephritis;
gynecomastia;
sweating;
peripheral edema;
microscopic colitis;
hypomagnesemia.

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

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.

Application in 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.

Use in 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 a trace of blood or melena), and if there is a stomach ulcer (or suspected gastric ulcer), the presence of a malignant tumor treatment with the drug Losek Maps may lead to a smoothing of symptoms and delay the diagnosis.

It is not recommended the joint use of omeprazole with such drugs as atazanavir and nelfinavir.

Pharmacokinetic / pharmacodynamic interaction between Clopidogrel (loading dose of 300 mg and maintenance dose of 75 mg per day) and omeprazole (80 mg per day orally) was noted on the results of the studies.which leads to a decrease in exposure to 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, 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 other similar studies have not shown an increased risk.

In randomized, double-blind, controlled clinical trials of omeprazole and esomeprazole, including two open trials with a duration of therapy of more than 12 years, the connection of fractures against osteoporosis with proton pump inhibitors was not confirmed.

Although the causal relationship between the use of omeprazole / esomeprazole with fractures against osteoporosis is not established, patients with a risk of developing osteoporosis or fractures against it should be under appropriate clinical supervision.

Impact on the ability to drive a car or other machinery

There is no evidence of the effect of Losek Mups on the ability to drive a car or other mechanisms. However, due to the fact that during therapy there may be dizziness, blurred vision and drowsiness, care should be taken when driving vehicles or other mechanisms.

Drug Interactions

Effect of omeprazole on the pharmacokinetics of other drugs

The decrease in the secretion of hydrochloric acid in the stomach in the treatment with omeprazole and other inhibitors of the proton pump can lead to a decrease or increase in the absorption of other drugs, the absorption of which depends on the acidity of the medium.

Like other drugs that reduce the acidity of gastric juice, treatment with omeprazole may lead to a decrease in absorption of ketoconazole, Itraconazole and erlotinib, and also an increase in the absorption of drugs such as digoxin.

Joint reception of omeprazole at a dose of 20 mg once a day and Digoxin increases the bioavailability of digoxin by 10% (bioavailability of digoxin was increased by up to 30% in 20% of patients).

It has been shown that omeprazole interacts with some antiretroviral drugs.

The mechanisms and the clinical significance of these interactions are not always known. An increase in pH on the background of omeprazole therapy may affect the absorption of antiretroviral drugs. It is also possible to interact at the level of the isoenzyme CYP2C19. 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 application Loseka saquinavir and saquinavir increase was observed in serum, when used with some other antiretroviral drugs, their concentration was not changed.

Omeprazole inhibits CYP2C19, the main isoenzyme 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 that patients who take phenytoin and omeprazole be monitored, a reduction in the dose of phenytoin may be required. However, concomitant treatment with omeprazole at a daily dose of 20 mg does not affect the concentration of phenytoin in the blood plasma in patients taking the drug for a long time. When omeprazole is used by patients receiving warfarin or other antagonists of vitamin K, monitoring of the international normalized relationship is necessary; in some cases, a dose reduction of warfarin or another vitamin K antagonist may be necessary. At the same time, the concomitant treatment with omeprazole at a daily dose of 20 mg does not lead to a change in coagulation time in patients taking warfarin for a long time.

The use of Losec in a dose of 40 mg once a day led 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. Pharmacokinetic / pharmacodynamic interaction between clopidogrel (loading dose of 300 mg and maintenance dose of 75 mg per day) and omeprazole (80 mg per day orally) was noted on the results of the studies.which leads to a decrease in exposure to the active metabolite of clopidogrel, on average, by 46% and a decrease in the maximum inhibition of ADP-induced platelet aggregation, on average, by 16%.

The clinical significance of this interaction is not clear. An increased risk of cardiovascular complications with the combined use of clopidogrel and proton pump inhibitors, including omeprazole, has not been shown in a prospective, randomized, unfinished study involving more than 3,760 patients who received placebo or omeprazole at a dose of 20 mg per day concomitantly with clopidogrel and acetylsalicylic therapy acid (ASA), and is not confirmed by an additional non-randomized analysis of clinical outcomes of large-scale prospective randomized trials involving more than 4 7000 patients.

The results of several observational studies are contradictory and do not give an unambiguous answer about the presence or absence of an increased risk of thromboembolic cardiovascular complications against the background of joint use of clopidogrel and proton pump inhibitors.

When clopidogrel is used together with a fixed combination of 20 mg of esomeprazole and 81 mg of ASA, exposure to the activethe metabolite of clopidogrel decreased by almost 40% compared to clopidogrel monotherapy, with the maximum levels of inhibition of ADP-induced platelet aggregation being the same, which is probably due to concomitant use of low-dose ASA.

Omeprazole does not affect the metabolism of drugs metabolized by the isoenzyme CYP3A4, such as, cyclosporine, lidocaine, quinidine, estradiol, Erythromycin and budesonide.

There was no interaction of omeprazole with the following drugs: caffeine, theophylline, S-varafarine, piroxicam, diclofenac, naproxen, metoprolol, propranolol, and ethanol (alcohol).

With the simultaneous use of omeprazole and tacrolimus, there was an increase in the concentration of tacrolimus in the blood serum.

Some patients reported increased concentrations of Methotrexate against a background of combined use with proton pump inhibitors. When appointing high doses of methotrexate, consideration should be given to the temporary discontinuation of Losek.

The effect of drugs on the pharmacokinetics of omeprazole

The isoenzymes CYP2C19 and CYP3 A4 are involved in the metabolism of omeprazole.The combined use of omeprazole and inhibitors of the CYP2C19 and CYP3A4 isoenzymes, such as clarithromycin and voriconazole, may increase the concentration of omeprazole in the blood plasma by slowing the metabolism of omeprazole. The combined use of voriconazole and omeprazole results in a more than two-fold increase in omeprazole AUC. Due to the good tolerability of high doses of omeprazole, with a short co-administration of these drugs, no dosage adjustment of omeprazole is required.

Drugs that induce isoenzymes CYP2C19 and CYP3A4, such as rifampicin and preparations of St. John's wort, when administered together with omeprazole, can lead to a decrease in the concentration of omeprazole in the blood plasma by accelerating the metabolism of omeprazole.

Analogues of medicinal product Losek

Structural analogs for the active substance:

Gastrozole;
Demeprazole;
Zhelezolic;
A zerocide;
Zolser;
Chrismel;
Losek the Map;
Omez;
Omez Insta;
Omesol;
Omeprazole;
Omepros;
Omeface;
Omizak;
OmiPix;
Omitox;
Ortanol;
Ozid;
Pepticum;
Pleom 20;
Pomez;
Romesque;
Ulzol;
Ulcozol;
Ultop;
Helicid;
Helol;
Cisagast.

Analogues for the pharmacological group (proton pump inhibitors):

Acrylase;
Beret;
Vimovo;
Dexylant;
A zerocide;
Zipantola;
Zolispan;
Zolser;
Zulbeks;
Controllers;
Chrismel;
Crosatide;
Lanzabel;
Lanzap;
Lansoptol;
Lansoprazole;
Lansofed;
Lancid;
Losek the Map;
Nexium;
Neo Sextus;
Nolpaz;
Нофлюкс;
Omez D;
Omeprazole;
Ontime;
Ortanol;
Pantaz;
Pantoprazole;
Panum;
Parries;
Pepazol;
Pepticum;
Pylobact;
Puloreph;
Rabelock;
Rabeprazole;
Razo;
Sunpras;
Ulter;
Hirabesol;
Helithrix;
Esomeprazole;
Emanera;
Epicurus.

If there are no analogues of the medication for the active substance, you can go to the links below for diseases, from which the corresponding drug helps, and to look at the available analogs for therapeutic effects.

Used for the treatment of diseases: ulcer, gastritis, esophagitis, reflux, Helicobacter, erosion, duodenal ulcer, dyspepsia, gerb, gastric ulcer, reflux esophagitis, erosion of the stomach, Zollinger-Ellison syndrome, gastroesophageal reflux disease, peptic ulcer