Content

According to the medical classification of drugs, Rabeprazole belongs to antiulcer drugs, proton pump inhibitors. This action is ensured by the fact that the product contains sodium rabeprazole. The medication is produced by the Russian pharmaceutical company Severnaya Zvezda. Check out its instructions for use.

Composition and form of release

Rabeprazole tablets have the following composition:

Pharmacological properties

Rabeprazole is an antisecretory drug that contains a benzimidazole derivative. The drug blocks the last stage of basal and stimulated production of hydrochloric acid, regardless of the stimulus.

Rabeprazole sodium is highly lipophilic, penetrates into cells, concentrates in them, increases the production of bicarbonate, and has a cytoprotective effect. The effect after taking the drug comes in an hour, reaches a maximum after 3 hours, lasts up to 23-48 hours. After the cancellation of the intake, activity is restored in 1-2 days. While taking Rabeprazole, the spread of Helicobacter pylori infection was not detected.

The agent is rapidly absorbed in the intestines, has 52% bioavailability with an hour half-life. With chronic liver damage, pharmacokinetics slows down. The properties of the drug are not affected by the time of its administration, the simultaneous use of antacids or fatty foods. Rabeprazole combines with plasma proteins by 97%, 90% of the dose is excreted in the urine in the form of metabolites - carboxylic acid and mercapturic acid conjugate.

Indications for use

The instruction highlights the indications for the use of the product:

• exacerbation of stomach ulcers, duodenal ulcers, anastomotic ulcer;
• non-erosive, erosive and ulcerative gastroesophageal reflux disease;
• reflux esophagitis in adults and children over 12 years old;
• Zollinger-Ellison syndrome, pathological hypersecretion;
• eradication of Helicobacter pylori combined with antibacterial therapy.

Method of administration and dosage

The instructions for use of Rabeprazole indicate that the capsules are swallowed whole. For stomach ulcers, take 10-20 mg once a day for a course of 6 weeks. The duration of treatment can be increased by another 6 weeks if the effect is insufficient. With an exacerbation of a duodenal ulcer, take 20 mg once a day (sometimes 10 mg is prescribed) for a course of 2-4 weeks.

To eliminate the symptoms of erosive gastroesophageal reflux disease, take 10-20 mg once a day for 4-8 weeks, non-erosive - 10-20 mg for 4 weeks. After relief of symptoms, maintenance therapy is 10 mg per day. For the treatment of hypersecretion, they begin with taking 60 mg per day, then the dose is increased to 100 mg per day or 60 mg twice a day for a course of up to a year. To eradicate Helicobacter pylori, take 20 mg twice a day for a weekly course. Children can be given 20 mg per day for 8 weeks.

special instructions

In the instructions, it is useful to study the special instructions section:

1. There is no data on the safety of using the product during pregnancy. Animal studies have shown that the active ingredient does not affect fertility. During pregnancy and lactation, it is better to refuse to take the drug.
2. Before therapy, the presence of malignant neoplasms in the stomach should be excluded.
3. While taking the drug, cases of hypomagnesemia are rarely observed. Of the serious side effects, arrhythmia, tetany, convulsions are also noted. Patients receiving digoxin and diuretics should be monitored for magnesium in the blood.
4. Treatment with medication increases the risk of osteoporosis, fractures of the hips, spine, and wrist.
5. Drug therapy can lead to an increased risk of infections caused by salmonella, campylobacter, clostridia.
6. It is unlikely that the product will adversely affect the vehicle's ability to drive. If the patient is drowsy, it is best not to drive.

Drug interactions

The instructions for use indicate the drug interaction of the drug:

1. It slows down the excretion of Diazepam, indirect anticoagulants, Phenytoin.
2. The agent reduces the concentration of Ketoconazole. Itraconazole in the blood.
3. The drug reduces the effect of Atanazavir, so this combination is prohibited.
4. It inhibits the metabolism of Cyclosporine, Theophylline.
5. Simultaneous administration of the drug with methotrexate increases the toxicity of the latter.
6. Amoxicillin, Clarithromycin, Warfarin increase the concentration of Rabeprazole in the blood.
7. There is no interaction between the drug and antacid suspensions based on magnesium hydroxide, aluminum.

Rabeprazole and alcohol

According to doctors, it is undesirable to combine Rabeprazole with alcohol, because the active ingredient is processed by the liver, which, when taking alcohol, experiences a double load. When the drug is combined with ethanol, the side effects may increase.

Side effects

When taking Rabeprazole, side effects may occur:

• swelling of the face, shortness of breath, hypotension;
• leukopenia, thrombocytopenia, neutropenia;
• anorexia, hyponatremia, hypomagnesemia;
• insomnia, headache, drowsiness, dizziness, nervousness, confusion, depression;
• visual impairment;
• pharyngitis, bronchitis, sinusitis, cough, rhinitis;
• diarrhea, abdominal pain, taste disturbances, flatulence, gastritis, nausea, stomatitis, vomiting, dry mouth, constipation, belching, dyspepsia, loss of appetite;
• fever;
• jaundice, hepatitis, encephalopathy, increased activity of liver enzymes;
• bullous eruptions, erythema, urticaria, necrolysis;
• nephritis, a urinary tract infection;
• myalgia, convulsions, arthralgia, bone fracture;
• gynecomastia;
• asthenia;
• infections.

Contraindications

The drug is prescribed with caution in renal and hepatic insufficiency. Contraindications are:

• intolerance to the components of the drug, substituted benzimidazoles;
• pregnancy;
• deficiency of sucrase-isomaltase;
• breast-feeding;
• children under 12 years of age.

Terms of sale and storage

The drug belongs to prescription, it is stored at temperatures up to 25 degrees for three years, away from children.

Analogs

Means with the same effect, the same or different composition, are capable of replacing the medication. Rabeprazole analogs:

• Zolispan, Ontaym, Noflux, Zulbeks - tablets based on rabeprazole.
• Khairabezole - capsules containing rabeprazole.

Rabeprazole or Omeprazole - which is better

Unlike Rabeprazole, Omeprazole contains another active substance that has a lower acidic range. Because of this, it takes twice as much medicine. Omeprazole has a higher risk of adverse reactions, loss of activity when taken after meals. Rabeprazole has a slower recovery period to the original acidity, there is no withdrawal syndrome. Omeprazole is cheaper. Rabeprazole is the more effective drug, so it is better.

Price

The cost of the drug in Moscow:

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A drug Rabeprazole- a remedy for the treatment of peptic ulcers and gastroesophageal reflux disease, a proton pump inhibitor.

Antisecretory, antiulcer agent - inhibitor of H +, K + - ATPase ("proton pump"). It accumulates and becomes active in the acidic environment of the secretory tubules of the parietal cells of the gastric mucosa. The active metabolite - sulfenamide - inhibits (partially reversibly) H +, K + - ATPase, stopping the release of hydrogen ions into the stomach cavity, which leads to blocking the final stage of hydrochloric acid secretion. Dose-dependently inhibits both basal and stimulated secretion, total gastric secretion and pepsin secretion. Has a bactericidal effect against Helicobacter pylori (the minimum inhibitory concentration is 4-16 μg / ml), accelerates the manifestation of the anti-Helicobacter activity of a number of antibiotics.

After a single dose of 20 mg of rabeprazole, inhibition of gastric secretion develops within 1 hour and reaches a maximum after 2-4 hours (after taking the first dose). The duration of inhibition of basal and stimulated secretion reaches 48 hours, a stable antisecretory effect develops after 3 days of treatment. The ability of parietal cells to produce hydrochloric acid is restored within 2-3 days after the end of therapy as new molecules of H +, K + - ATPase are synthesized, the cancellation is not accompanied by the phenomenon of "rebound". Rabeprazole in combination with antibiotics ensures the eradication of Helicobacter pylori in 90% of patients within 4 days.

Pharmacokinetics.

After ingestion, absorption begins in the small intestine (due to the presence of an acid-fast enteric coating in the tablet) and is carried out quickly and completely. Bioavailability is 52% due to the pronounced effect of the "first pass" through the liver; concurrent food intake does not affect bioavailability. Plasma protein binding is 95%. In the dose range of 10-40 mg, the bioavailability and maximum concentration of rabeprazole are linearly dose dependent. After taking 20 mg of rabeprazole, the maximum plasma concentration is reached, on average, after 3.5 hours. It is metabolized in the liver with the participation of isoenzymes of the cytochrome P450 system (CYP2C19 and CYP3A) with the formation of inactive metabolites and demethylthioester, which has a weak antisecretory activity. The half-life is 0.7-1.5 hours, the total clearance is 283 ml / min. It is excreted mainly by the kidneys in the form of metabolites - conjugates of mercapturic and carboxylic acids.

In liver diseases, the bioavailability of rabeprazole increases 2 times (after a single dose) and 1.5 times (after 7 days of therapy), the half-life increases to 12.3 hours.

In the case of delayed biotransformation after 7 days of taking in a daily dose of 20 mg, the maximum concentration increases by 40%, the half-life is, on average, 1.6 hours.

At the stage of end-stage renal failure in patients on dialysis, pharmacokinetic parameters change insignificantly: the maximum concentration and bioavailability decrease by 35%, the half-life during hemodialysis is 0.95 hours, after - 3.6 hours.

In elderly patients, the maximum concentration in the blood increases by 60%, bioavailability doubles, and elimination slows down.

Indications for use

• active peptic ulcer of the duodenum;
• active benign stomach ulcer;
• erosive or ulcerative gastroesophageal reflux disease (GERD);
• long-term treatment of gastroesophageal reflux disease (maintenance therapy for GERD);
• symptomatic treatment of moderate to very severe gastroesophageal reflux disease (symptomatic treatment of GERD);
• Zollinger-Ellison syndrome;
• in combination with appropriate antibacterial therapeutic regimens for the eradication of Helicobacter pylori (H. pylori) in patients with peptic ulcers of the stomach and duodenum.

Mode of application

Adults and elderly patients.

Active peptic duodenal ulcer and active benign gastric ulcer: The recommended dose for these diseases is 20 mg once daily in the morning.

In most patients with active peptic ulcer of the duodenum, the time required for the ulcer to heal is up to 4 weeks.

It should be noted, however, that some patients should take Rabeprazole-Health additionally for another 4 weeks. Most patients with active benign gastric ulcer heal within 6 weeks, but some patients who are not responsive to treatment should take Rabeprazole-Health for an additional 6 weeks to heal ulcers.

Erosive or ulcerative gastroesophageal reflux disease: The recommended dose for these diseases is 20 mg 1 time per day for 4-8 weeks.

Long-term treatment of gastroesophageal reflux disease (GERD maintenance therapy):

for long-term use, you can use maintenance doses of Rabeprazole-Health 10 mg or 20 mg 1 time per day (dose depending on the effectiveness of treatment).

Symptomatic treatment of GERD: for patients without esophagitis, Rabeprazole-Health is prescribed at a dose of 10 mg once a day. If symptoms persist after 4 weeks of treatment, additional examination of the patient should be performed. Once symptoms have disappeared, follow-up control of symptoms can be achieved using an “on demand” regimen: 10 mg once daily as needed.

Zollinger-Ellison syndrome: the dose is selected individually. The initial dose is 60 mg per day. A single dose of up to 100 mg per day can be used. If necessary, the dose is increased and the drug is prescribed in a dose of up to 120 mg per day with a single dose or 60 mg 2 times a day. Treatment is continued if clinically necessary. The duration of the course of treatment and the dosage regimen are determined individually.

Eradication of H. pylori: in patients with H. pylori, appropriate combinations of Rabeprazole-Health with antibiotics should be used. Recommended appointment within 7 days:

Rabeprazole-Zdorov'e 20 mg 2 times a day + clarithromycin 500 mg 2 times a day and amoxicillin 1 g 2 times a day.

According to indications that require taking only once a day, Rabeprazole-Health tablets should be taken in the morning before meals. Although morning or mealtime has not been shown to affect rabeprazole sodium, this regimen is more beneficial for treatment. The tablets should not be chewed or crushed, but must be swallowed whole.

Impaired kidney and liver function. Patients with impaired renal or hepatic function do not need dose adjustment Rabeprazole-Health... Application in the treatment of patients with severely impaired liver function is discussed in more detail in the section "Peculiarities of use".

Side effects

In clinical trials Rabeprazole-Health well tolerated by patients. The side effects that were observed were mostly minor, moderate and quickly resolved. The most common negative symptoms are headache, diarrhea and nausea. Adverse reactions, which were observed more often, are listed below by organ systems and frequency.

The following adverse reactions have been observed during clinical studies. However, of these adverse reactions that were observed during clinical trials, only headache, diarrhea, abdominal pain, asthenia, flatulence, rash and dry mouth were associated with the use of Rabeprazole-Health.

Infections and infestations. Often infections.

Blood and lymphatic system. Rarely - neutropenia, leukopenia, thrombocytopenia, leukocytosis.

From the immune system. Rarely - hypersensitivity reactions (including facial edema, arterial hypotension and dyspnea; erythema, bullous reactions and acute systemic allergic reactions, which usually disappear after stopping treatment).

From the side of metabolism. Rarely - anorexia. Unknown - hyponatremia.

Mental disorders. Often insomnia. Uncommon - nervousness. Rarely depression. Unknown - confusion.

From the nervous system. Often - headache, dizziness. Infrequently - drowsiness.

On the part of the organ of vision. Rarely - visual disturbances.

Vascular Disorders. Unknown - peripheral edema.

From the respiratory system. Often - cough, pharyngitis, rhinitis. Infrequently - bronchitis, sinusitis.

From the digestive tract. Often - diarrhea, vomiting, nausea, abdominal pain, constipation, flatulence. Infrequently - indigestion, dry mouth, belching. Rarely - gastritis, stomatitis, impaired sense of taste.

Disorders of the liver and biliary tract. Rarely - hepatitis, jaundice, hepatic encephalopathy (in isolated cases, hepatic encephalopathy was observed in patients with cirrhosis).

On the part of the skin and subcutaneous tissues. Infrequently - rash, erythema (bullous reactions and acute systemic allergic reactions, which usually disappear after stopping treatment). Rarely - itching, sweating, bullous reactions. Very rarely - erythema multiforme, toxic epidermal necrosis (TEN), Stevens-Johnson syndrome.

From the musculoskeletal system. Often nonspecific / back pain. Uncommon - myalgia, leg cramps, arthralgia.

On the part of the kidneys and urinary system. Uncommon - urinary tract infections. Rarely, interstitial nephritis.

On the part of the reproductive system. Unknown - gynecomastia.

General disorders and uses. Often - asthenia, flu-like syndrome. Uncommon - chest pain, chills, fever.

Research. Infrequently - an increase in the level of liver enzymes. Rarely - an increase in body weight.

Contraindications

Contraindications to the use of the drug Rabeprazole are: the presence of a malignant process in the stomach and duodenum, pregnancy, lactation, individual hypersensitivity to rabeprazole, other components of the drug, substituted benzimidazoles.

Pregnancy

Studies of the safety of the use of rabeprazole in pregnant women have not been conducted, therefore the use of Rabeprazole-Health contraindicated in pregnancy. It is not known whether rabeprazole sodium is excreted in breast milk. No relevant studies have been carried out, therefore Rabeprazole-Health should not be administered to women during lactation.

Interaction with other medicinal products

Rabeprazole sodium causes a strong and long-term decrease in gastric acid production. Thus, sodium rabeprazole, in principle, can interact with drugs, the absorption of which depends on the pH of the gastric contents. The simultaneous use of rabeprazole sodium and ketoconazole or itraconazole can lead to a significant decrease in plasma levels of these antifungal agents.

Thus, individual patients who use these drugs together with Rabeprazole-Zdorovye should be monitored to determine the need for dose adjustment. In clinical trials, patients simultaneously with Rabeprazole-Health took antacids if necessary; in a special study, the interaction of Rabeprazole-Health with an antacid, which is taken in liquid form, was not observed.

Concomitant use of atazanavir 300 mg / ritonavir 100 mg with omeprazole (40 mg once daily) or atazanavir 400 mg with lansoprazole (60 mg once daily) in healthy volunteers resulted in a significant decrease in atazanavir exposure. Absorption of atazanavir is pH dependent, therefore proton pump inhibitors, including rabeprazole, should not be used in combination with atazanavir.

Overdose

Experience of intentional or accidental overdose Rabeprazole limited. The maximum reported effect did not exceed 60 mg twice a day or 160 mg once a day. In general, the effect is minimal, typical for known adverse reactions and circulating without subsequent medical effects. The specific antidote for Rabeprazole-Health is unknown. Rabeprazole sodium binds well to plasma proteins and is not excreted during dialysis. In case of overdose, symptomatic and supportive treatment is necessary.

Storage conditions

Additionally

Symptomatic improvement in response to rabeprazole therapy can also occur in the presence of a malignant neoplasm of the stomach, and therefore, before starting therapy with Rabeprazole-Health, it is necessary to exclude the possibility of tumors. Patients with a long course of treatment (especially those who have been treated for more than one year) should be monitored regularly.

The risk of cross-hypersensitivity with other proton pump inhibitors or substituted benzimidazoles is not excluded.

Patients should be warned that Rabeprazole-Health tablets should not be chewed or crushed, but should be swallowed whole.

There were post-marketing reports of pathological changes in the blood (thrombocytopenia and neutropenia). In most cases, no other etiology was found; the cases were uncomplicated and disappeared after discontinuation of rabeprazole.

In clinical studies, abnormal liver enzymes have been observed and there have also been reports in the post-marketing period. In most cases, no other etiology was found; the cases were uncomplicated and disappeared after discontinuation of rabeprazole.

In a special study in patients with mild or moderate impairment of liver function, there was no significant cancellation of the frequency of side effects when taking Rabeprazole-Health compared with a control group of the corresponding sex and age.

The doctor should be careful when prescribing the drug in the early stages of therapy for patients with severe renal impairment, since there are no clinical data regarding the use of the drug by patients in this group.

The simultaneous use of atazanavir and Rabeprazole-Zdorovye is not recommended (see the section "Interaction with other medicinal products and other types of interactions").

Considering the pharmacodynamics of rabeprazole sodium and its inherent profile of side effects, it can be assumed that Rabeprazole-Health should not negatively affect driving and work with potentially dangerous mechanisms. At the same time, in case of drowsiness, it is recommended to avoid driving and work with other mechanisms.

Main settings

Name:

RABEPRAZOLE

Catad_pgroup Antisecretory, proton pump inhibitors

Rabeprazole 20mg - instructions for use

Registration number:

LP-005191

Trade name:

Rabeprazole

International non-proprietary name:

rabeprazole

Dosage form:

enteric coated tablets

Compound

1 enteric coated tablet 20 mg contains:
Tablet core composition:
Active substance: rabeprazole sodium - 20.0 mg, corresponds to rabeprazole - 18.85 mg.
Excipients: magnesium oxide, low-substituted hyprolose (hydroxypropyl cellulose), mannitol, hypromellose, sodium stearyl fumarate.
Tablet 1 shell composition: opadry colorless 03K19229 (hypromellose, triacetin, talc), magnesium oxide.
Tablet 2 shell composition: shureliz colorless E-7-19040 (ethylcellulose, ammonium hydroxide, medium-chain triglycerides, oleic acid).
Tablet shell composition 3: acrylysis II yellow 493Z220000 (methacrylic acid and ethyl acrylate copolymer (1: 1), talc, titanium dioxide, poloxamer 407, calcium silicate, sodium bicarbonate, sodium lauryl sulfate, iron dye yellow oxide).

Description

Tablets 20 mg: tablets are round, biconvex, coated from light yellow to yellow.

Pharmacotherapeutic group:

an agent that lowers the secretion of gastric glands - a proton pump inhibitor.

ATX code:

Pharmacological properties

Pharmacodynamics
Mechanism of action
Rabeprazole sodium belongs to the class of antisecretory substances derived from benzimidazole. Rabeprazole sodium suppresses gastric acid secretion by specifically inhibiting H + / K + ATPase on the secretory surface of gastric parietal cells. The H + / K + ATPase is a protein complex that functions as a proton pump, thus rabeprazole sodium is a proton pump inhibitor in the stomach and blocks the final stage of acid production. This effect is dose-dependent and leads to the suppression of both basal and stimulated acid secretion, regardless of the stimulus. Rabeprazole sodium has no anticholinergic properties.
Anti-secret action
After oral administration of 20 mg of rabeprazole sodium, the antisecretory effect develops within an hour. Inhibition of basal and stimulated acid secretion 23 hours after taking the first dose of rabeprazole sodium is 69% and 82%, respectively, and lasts up to 48 hours. This duration of pharmacodynamic action is much longer than predicted based on the half-life (approximately one hour). This effect can be explained by the prolonged binding of the drug to the H + / K + ATPase of gastric parietal cells. The magnitude of the inhibitory effect of rabeprazole sodium on acid secretion reaches a plateau after three days of administration of rabeprazole sodium. When you stop taking, secretory activity is restored within 1-2 days.
Effect on plasma gastrin levels
In clinical trials, patients received 10 or 20 mg of rabeprazole sodium daily for up to 43 months of treatment. Plasma gastrin levels were elevated during the first 2–8 weeks, reflecting an inhibitory effect on acid secretion. The gastrin concentration returned to baseline, usually within 1–2 weeks after discontinuation of treatment.
Effect on enterochromaffin-like cells
In the study of biopsy samples of the human stomach from the antrum and fundus of the stomach of 500 patients who received rabeprazole sodium or a reference drug for 8 weeks, persistent changes in the morphological structure of enterochromaffin-like cells, the severity of gastritis, the frequency of atrophic gastritis, intestinal metaplasia or the spread of infection Helicobacter pylori were not found.
In a study of over 400 patients treated with rabeprazole sodium (10 mg / day or 20 mg / day) for up to 1 year, the incidence of hyperplasia was low and comparable to that of omeprazole (20 mg / kg). There were no reported cases of adenomatous changes or carcinoid tumors observed in rats.
Other effects
Systemic effects of rabeprazole sodium on the central nervous system, cardiovascular or respiratory systems have not been detected at the moment. It has been shown that oral administration of rabeprazole sodium at a dose of 20 mg for 2 weeks does not affect the function of the thyroid gland, carbohydrate metabolism, the level of parathyroid hormone in the blood, as well as the level of cortisol, estrogen, testosterone, prolactin, glucagon, follicle-stimulating hormone (FSH), luteinizing hormone (LH), renin, aldosterone and growth hormone.

Pharmacokinetics
Absorption
Rabeprazole is rapidly absorbed from the intestine, and peak plasma concentrations are reached approximately 3.5 hours after a 20 mg dose. Changes in peak plasma concentrations (C max) and values ​​of the area under the concentration-time curve (AUC) of rabeprazole are linear in the dose range from 10 to 40 mg. The absolute bioavailability after oral administration of 20 mg (compared to intravenous administration) is about 52%. In addition, the bioavailability does not change with repeated administration of rabeprazole. In healthy volunteers, the plasma half-life is about 1 hour (varying from 0.7 to 1.5 hours), and the total clearance is 3.8 ml / min / kg. In patients with chronic liver damage, the AUC is doubled compared with healthy volunteers, which indicates a decrease in first-pass metabolism, and the plasma half-life is increased by 2-3 times. Neither the time of taking the drug during the day nor antacids affect the absorption of rabeprazole. Taking the drug with fatty foods slows down the absorption of rabeprazole by 4 hours or more, but neither C max, nor the degree of absorption change.
Distribution
In humans, the degree of binding of rabeprazole to plasma proteins is about 97%.
Metabolism and excretion
In healthy people
After taking a single oral dose of 20 mg of 14 C-labeled sodium rabeprazole, no unchanged drug was found in urine. About 90% of rabeprazole is excreted in the urine mainly in the form of two metabolites: the conjugate of mercapturic acid (M5) and carboxylic acid (M6), as well as in the form of two unknown metabolites identified during toxicological analysis. The remainder of the sodium rabeprazole taken is excreted in the feces.
The total elimination is 99.8%. These data indicate a small excretion of sodium rabeprazole metabolites in the bile. The main metabolite is thioether (M1). The only active metabolite is desmethyl (M3), but it was observed at low concentrations in only one study participant after taking 80 mg of rabeprazole.
End stage renal disease
In patients with stable end-stage renal disease who require maintenance hemodialysis (creatinine clearance<5 мл/мин/1,73 м²), выведение рабепразола натрия схоже с таковым для здоровых добровольцев. AUC и С max у этих пациентов было примерно на 35% ниже, чем у здоровых добровольцев. В среднем период полувыведения рабепразола составлял 0,82 ч у здоровых добровольцев, 0,95 ч у пациентов во время гемодиализа и 3,6 ч после гемодиализа. Клиренс препарата у пациентов с заболеваниями почек, нуждающихся в гемодиализе, был приблизительно в два раза выше, чем у здоровых добровольцев.
Chronic compensated cirrhosis
Patients with chronic compensated liver cirrhosis tolerate rabeprazole sodium at a dose of 20 mg 1 time per day, although the AUC is doubled and C max is increased by 50% compared to healthy volunteers of the corresponding sex.
Elderly patients
Elimination of rabeprazole is somewhat slower in elderly patients. After 7 days of taking rabeprazole 20 mg per day, the AUC was approximately twice as high in the elderly, and the C max was increased by 60% compared with young healthy volunteers. However, there were no signs of cumulation of rabeprazole.
CYP2C19 polymorphism
In patients with a slow metabolism of CYP2C19, after 7 days of taking rabeprazole at the house of 20 mg per day, AUC increases 1.9 times, and the half-life increases 1.6 times compared with the same parameters in "fast metabolizers", while C max increases by 40%.

Indications for use

• Peptic ulcer in the acute stage and anastomotic ulcer;
• Duodenal ulcer in the acute stage;
• Erosive and ulcerative gastroesophageal reflux disease or reflux esophagitis;
• Maintenance therapy for gastroesophageal reflux disease;
• Non-erosive gastroesophageal reflux disease;
• Zollinger-Ellison syndrome and other conditions characterized by pathological hypersecretion;
• In combination with appropriate antibiotic therapy for eradication Helicobacter pylori in patients with peptic ulcer disease.

Contraindications

• Hypersensitivity to rabeprazole, substituted benzimidazoles or to any of the excipients of the drug;
• Pregnancy;
• Breastfeeding period;
• Age up to 12 years.

Carefully

• Childhood;
• Severe renal failure.

Application during pregnancy and during breastfeeding

There are no data on the safety of using rabeprazole during pregnancy. Reproductive studies in rats and rabbits showed no signs of impaired fertility or fetal developmental defects due to rabeprazole; however, in rats, in small amounts, the drug crosses the placental barrier. Rabeprazole should not be used during pregnancy unless the expected benefit to the mother outweighs the potential harm to the fetus.
It is not known whether rabeprazole is excreted in breast milk. Appropriate studies have not been conducted in lactating women. However, rabeprazole is found in the milk of lactating rats, and therefore rabeprazole should not be prescribed to lactating women.

Method of administration and dosage

Rabeprazole tablets should not be chewed or crushed. The tablets should be swallowed whole. It was found that neither time of day nor food intake affects the activity of rabeprazole sodium
With gastric ulcer in the acute stage and anastomotic ulcer it is recommended to take 20 mg orally once a day. Usually, cure occurs after 6 weeks of therapy, but in some cases, the duration of treatment can be increased by another 6 weeks.
With peptic ulcer of the duodenum in the acute stage it is recommended to take 20 mg orally once a day. The duration of treatment is 2 to 4 weeks. If necessary, the duration of treatment can be increased by another 4 weeks.
When treating erosive gastroesophageal reflux disease or reflux esophagitis it is recommended to take 20 mg orally once a day. The duration of treatment is 4 to 8 weeks. If necessary, the duration of treatment can be increased by another 8 weeks.
With maintenance therapy of gastroesophageal reflux disease it is recommended to take 20 mg orally once a day. The duration of treatment depends on the patient's condition.
For non-erosive gastroesophageal reflux disease without esophagitis it is recommended to take 20 mg orally once a day. If symptoms persist after four weeks of treatment, additional testing of the patient should be performed. After relief of symptoms, to prevent their subsequent occurrence, the drug should be taken orally once a day on demand.
For the treatment of Zollinger-Ellison syndrome and other conditions characterized by pathological hypersecretion, the dose is selected individually. The initial dose is 60 mg per day, then the dose is increased and the drug is prescribed in a dose of up to 100 mg per day with a single dose or 60 mg twice a day. For some patients, fractional dosing is preferred. Treatment should be continued as clinically necessary. In some patients with Zollinger-Ellison syndrome, the duration of treatment with rabeprazole was up to one year.
For the eradication of Helicobacter pylori it is recommended to take orally 20 mg 2 times a day according to a specific scheme with an appropriate combination of antibiotics. The duration of treatment is 7 days.
Patients with renal and hepatic impairment
No dose adjustment is required in patients with renal impairment.
In patients with mild to moderate hepatic impairment, the concentration of rabeprazole in the blood is usually higher than in healthy patients.
Caution should be exercised when prescribing rabeprazole to patients with severe hepatic impairment.
Elderly patients
No dose adjustment is required.
Children
The safety and efficacy of rabeprazole sodium 20 mg for the short-term (up to 8 weeks) treatment of gastroesophageal reflux disease in children aged 12 years and over has been confirmed by extrapolating the results of adequate and well-controlled studies supporting the efficacy of rabeprazole sodium for adults, and safety and pharmacokinetic studies in pediatric patients. age.
The recommended dose for children aged 12 years and over is 20 mg once a day for up to 8 weeks.
The safety and effectiveness of rabeprazole sodium for the treatment of gastroesophageal reflux disease in children under 12 years of age has not been established. The safety and efficacy of rabeprazole sodium for other indications has not been established in pediatric patients.

Side effect

To determine the incidence of side effects of the drug, the following classification is used: very often (≥1 / 10); often (≥1 / 100 and<1/10); нечасто (≥1/1000 и <1/100); редко (≥1/10000 и <1/1000); очень редко (<1/10000), включая единичные случаи.
Immune system disorders: rarely - acute systemic allergic reactions.
Blood and lymphatic system disorders: rarely - thrombocytopenia, neutropenia, leukopenia.
Metabolic and nutritional disorders: rarely - hypomagnesemia.
Liver and biliary tract disorders: increased activity of liver enzymes, rarely - hepatitis, jaundice, hepatic encephalopathy;
Kidney and urinary tract disorders: very rarely - interstitial nephritis.
Skin and subcutaneous tissue disorders: rarely - bullous rashes, urticaria; very rarely - erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome.
Musculoskeletal and connective tissue disorders: rarely - myalgia, arthralgia.
Genital and breast disorders: very rarely - gynecomastia. There were no changes in other laboratory parameters while taking rabeprazole sodium.
According to post-marketing data, taking proton pump inhibitors (PPIs) may increase the risk of fractures (see section "Special instructions").

Overdose

Symptoms
Data on intentional or accidental overdose are minimal. There have been no cases of severe overdose with rabeprazole.
Treatment
The specific antidote is unknown. Rabeprazole binds well to plasma proteins and is therefore poorly excreted during dialysis. In case of overdose, symptomatic and supportive treatment is necessary.

Interaction with other medicinal products

Cytochrome P450 system
Rabeprazole sodium, like other PPIs, is metabolized with the participation of the cytochrome P450 (CYP450) system in the liver. In research in vitro on microsomes of human liver, it was shown that sodium rabeprazole is metabolized by isoenzymes CYP2C19 and CYP3A4. Studies in healthy volunteers have shown that rabeprazole sodium has no pharmacokinetic or clinically significant interactions with drugs that are metabolized by the cytochrome P450 system - warfarin, phenytoin, theophylline and diazepam (regardless of whether patients metabolize diazepam intensively or weakly).
A study was conducted of combination therapy with antibacterial drugs. This four-way crossover study involved 16 healthy volunteers who received 20 mg rabeprazole, 1000 mg amoxicillin, 500 mg clarithromycin, or a combination of these drugs (CANCER - rabeprazole, amoxicillin, clarithromycin). AUC and C max values ​​for clarithromycin and amoxicillin were similar when comparing combination therapy with monotherapy. AUC and C max for rabeprazole increased by 11% and 34%, respectively, and for 14-hydroxyclarithromycin (an active metabolite of clarithromycin), AUC and C max increased by 42% and 46%, respectively, for combination therapy compared with monotherapy. This increase in exposure rates for rabeprazole and clarithromycin was not considered clinically significant.
Interaction due to inhibition of gastric acid secretion
Rabeprazole sodium provides stable and long-term suppression of gastric acid secretion. Thus, interactions can occur with substances for which the absorption depends on the pH. When taken simultaneously with rabeprazole sodium, the absorption of ketoconazole is reduced by 30%, and the absorption of digoxin is increased by 22%. Therefore, for some patients, observation should be carried out to resolve the issue of the need to adjust the dose while taking rabeprazole sodium with ketoconazole, digoxin, or other drugs for which absorption depends on pH.
Atazanavir
At the same time taking atazanavir 300 mg / ritonavir 100 mg with omeprazole (40 mg once a day) or atazanavir 400 mg with lansoprazole (60 mg once a day) in healthy volunteers, a significant decrease in the exposure to atazanavir was observed. The absorption of atazanavir is pH dependent. Although coadministration with rabeprazole has not been studied, similar results are expected for other PPIs as well. Therefore, concomitant use of atazanavir with PPIs, including rabeprazole, is not recommended.
Antacids
In clinical studies, antacids have been used in conjunction with sodium rabeprazole. No clinically significant interactions of rabeprazole sodium with aluminum hydroxide gel or magnesium hydroxide have been observed.
Eating
In a clinical study, no clinically significant interactions were observed with rabeprazole sodium with a low-fat diet. Taking rabeprazole sodium simultaneously with food enriched with fats can slow down the absorption of rabeprazole for up to 4 hours or more, however, C max and AUC do not change.
Cyclosporine
Experiments in vitro using human liver microsomes showed that rabeprazole inhibits the metabolism of cyclosporine with an IC 50 of 62 μmol, i.e. at a concentration 50 times higher than C max for healthy volunteers after 20 days of taking 20 mg of rabeprazole. The degree of inhibition is similar to that of omeprazole for equivalent concentrations.
Methotrexate
According to reports of adverse events, data from published pharmacokinetic studies and data from retrospective analysis, it can be assumed that the simultaneous use of PPIs and methotrexate (primarily in high doses) can lead to an increase in the concentration of methotrexate and / or its metabolite hydroxymethotrexate and increase the half-life. However, there have been no specific studies of drug interactions between methotrexate and PPIs.

special instructions

The patient's response to therapy with rabeprazole sodium does not exclude the presence of malignant neoplasms in the stomach.
Rabeprazole tablets should not be chewed or crushed. The tablets should be swallowed whole. It was found that neither the time of day nor food intake affects the activity of rabeprazole sodium.
In a special study in patients with mild to moderate liver dysfunction, no significant difference was found in the incidence of side effects of rabeprazole sodium from that in age-matched healthy individuals, but despite this, it is recommended to be careful when first administering rabeprazole sodium to patients with severe impaired liver function. The AUC of rabeprazole sodium in patients with severe hepatic dysfunction is approximately twice as high as in healthy volunteers.
Patients with impaired renal or hepatic function do not need to adjust the dose of rabeprazole.
Hypomagnesemia
Symptomatic and asymptomatic hypomagnesemia has rarely been reported with PPI treatment for at least 3 months. In most cases, these reports were received one year after therapy. Tetany, arrhythmias, and seizures were serious side effects. Most patients required treatment for hypomagnesemia, including magnesium replacement and discontinuation of PPI therapy. In patients who will be on long-term treatment or who are taking PPIs with drugs such as digoxin or drugs that can cause hypomagnesemia (such as diuretics), healthcare providers should monitor magnesium levels before starting PPI treatment and during treatment.
Patients should not take other acid-lowering agents, such as H2 blockers or PPIs, at the same time as rabeprazole.
Bone fractures
Observational studies suggest that PPI therapy may increase the risk of osteoporosis-related fractures of the hip, wrist, or spine. The risk of fractures was increased in patients who received high doses of PPIs for a long time (a year or more).
Concomitant use of rabeprazole with methotrexate
According to the literature, the simultaneous use of PPIs with methotrexate (primarily in high doses) can lead to an increase in the concentration of methotrexate and / or its metabolite hydroxymethotrexate and increase the half-life, which can lead to the toxicity of methotrexate. If high doses of methotrexate are required, temporary discontinuation of PPI therapy may be considered.
Clostridium difficile
PPI therapy may increase the risk of gastrointestinal infections such as Clostridium difficile.

Influence on the ability to drive vehicles and mechanisms

Based on the pharmacodynamic characteristics of rabeprazole and its profile of adverse effects, it is unlikely that it affects the ability to drive a car and work with equipment. However, if drowsiness occurs, these activities should be avoided.

Release form

Enteric coated tablets, 20 mg.
7, 10 or 14 tablets in a blister strip made of PVC film and aluminum foil or 14, 28, 30 or 60 tablets in a jar made of low-pressure polyethylene, sealed with a lid made of low-pressure polyethylene with first opening control (liner-insert on polymer and cardboard base) or without it.
1, 2, 4 or 8 blister packs of 7 tablets each, or 1, 2 or 4 blister packs of 14 tablets each, or 1, 2, 3, 5, 6, 9 or 10 blister packs of 10 tablets , or 1 can, together with instructions for medical use, are placed in a box made of cardboard box.

Storage conditions

In a dark place at a temperature not exceeding 25 ° C.
Keep out of the reach of children.

Best before date

2 years.
Do not use after the expiration date.

Vacation conditions

On prescription.

Manufacturer

Izvarino Pharma LLC,

Consumer claims should be sent to:

142750, Moscow, Izvarino village, VNTsMDL territory, p. 1.

"Rabeprazole" is a drug whose main action is performed by the substance of the same name. It is taken for gastroesophageal reflux, duodenal ulcer and stomach ulcer, effectively fights against microorganisms that provoke these diseases. If the patient is allergic to any component that contains "Rabeprazole", analogs may well replace this drug.

Description

The drug is used in a number of cases:

• with peptic ulcer of the duodenum and stomach in combination with some antibiotics;
• in the presence of Zollinger-Ellison syndrome;
• for the treatment of benign stomach ulcers;
• if you have GERD.

The course of admission lasts from one to eight weeks. If necessary, the treatment period is extended on an individual basis. If you take "Rabeprazole sodium" for therapeutic purposes, the analogs of which have similar characteristics, then in some cases you can observe the appearance of a number of side effects:

• backache,
• fever,
• rash,
• cough,
• rhinitis,
• convulsions
• myalgia,
• leukopenia,
• drowsiness,
• dizziness,
• flatulence,
• constipation,
• nausea,
• diarrhea.

The drug is prohibited for use in case of malignant tumors in the gastrointestinal tract, strong sensitivity to the components of the drug, pregnancy and lactation.

Analogs of "Rabeprazole"

"Rabeprazole", analogs of which are similar in pharmacological effect and application, can be replaced, if necessary, with one of the following drugs:

• "Novobismol".
• "Ontime".
• Omeprazole.
• "Ulkavis".
• "Lansobel".
• "Omegast".
• "Pantap".
• Famo.
• "Omez".
• "Dalargin".
• "Zolispan".
• "Zulbeks".
• "Peptipak".
• Magnagel.
• "Parastamik".
• Loseprazole.
• "Pariet".
• "Rabelok".
• "Noflux".
• Famotidine.

It is worth remembering that it is impossible to independently make a decision about taking another remedy, since only a qualified doctor will be able to give the best recommendations, taking into account the existing characteristics of the body and the patient's condition.

Features of the use of analogs

Before using "Rabeprazole", analogs, instructions for use should be read in full. Although drugs are prescribed for identical diseases, each of them still has characteristic features. For example, Omeprazole can cause nephritis, erythema, bronchospasm, stomatitis, candidiasis, hallucinations, and depression. Reception of "Famotidine" in some cases provokes acne, baldness, violation of heart contractions, mental disorders, tinnitus, jaundice, loss of appetite.

"Pariet" most often does not cause side effects. Rarely observed Stevens-Johnson syndrome, necrolysis, hypomagnesemia, edema, dry mouth, gynecomastia. It should not be prescribed not only to pregnant women and patients with high sensitivity to rabeprazole, but also to children under twelve years of age. "Magnagel" is allowed to give to children from the age of six. Its use is not capable of leading to serious consequences. Sometimes there are only problems with the gastrointestinal tract.

special instructions

In its pharmacological group, one of the cheapest medicines is Rabeprazole. Analogs, the price of which is higher in most cases, are used less frequently. Their cost varies from 135 to 3750 rubles on average in the country.

Before taking "Rabeprazole", you should know for sure that the patient does not have any malignant tumors in the gastrointestinal system, since the drug can interfere with the timely diagnosis of the pathology and, possibly, lead to its progression.

It is also worth making sure that the patient is not pregnant, as the medication has a negative effect on the developing baby. The drug can penetrate into the child's body through breast milk, therefore, during treatment, the woman must stop feeding the child.

If, after taking these pills, a person feels tired, then he will have to refuse to drive a car for the entire course of treatment. It should be remembered that some means used together have an effect on each other. For example, "Rabeprazole", the analogs of which are largely identical in their characteristics, must be carefully combined with "Digoxin", "Ketonazole", "Itraconazole" and "Atazanavir".

Comparison of analogues

A comparative table of analogs is as follows:

Name	Bioavailability percentage	Maximum concentration time in hours	Half-life in hours
"Rabeprazole"	52	three and a half - four	twenty four
"Rabelok"	34-50	two three	one and a half - two and a half
"Pariet"	67-73	six - eight	one - two and a half
"Ontime"	74-80	two - four	one to five
"Noflux"	65-70	three four	one to four
"Zulbeks"	68-74	three - six	one two
"Khairabezol"	43-54	four to eight	one and a half - two and a half
"Zolispan"	40-45	four five	one two

It is worth noting that the half-life of "Rabeprazole" is the longest among identical drugs. At the same time, it will take 3.5-4 hours to wait for its maximum concentration in the body. And this is much more than some substitutes.

So, for the treatment of ulcers in the duodenum and stomach, as well as for gastroesophageal disease and Zollinger-Ellison syndrome, "Rabeprazole" is successfully used. Analogs of the drug, if necessary, effectively replace it. However, only a doctor can offer specific treatment regimens.

The chemical composition of one enteric capsule of Rabeprazole contains 10 mg of an active drug compound rabeprazole sodium .

Release form

Enteric capsules (10 mg.), The number of which in one package can vary from 5 to 60 pieces.

pharmachologic effect

This drug belongs to the group antiulcer drugs , so-called, inhibitors of H + -K + -ATP-ase.

Pharmacodynamics and pharmacokinetics

This medicine has an effect on enzyme H + -K + -ATPase, which is produced in parietal cells of the stomach acting like proton pump inhibitor ... As a result, an actively acting drug compound blocks the formation of hydrochloric acid at the final stage, and also reduces stimulation secretions regardless of the type of stimulus.

After taking the drug at a dosage of 20 mg. complete absorption occurs after about 3.5 hours. It is noteworthy that bioavailability an active drug compound, as well as the absorbing properties of the drug itself, do not depend on the time of its administration.

Indications for use

The drug is used in the treatment of:

• , including at the stage of exacerbation of the disease;
• pathological hypersecretion ;
• gastroesophageal reflux disease ;
• Zollinger-Ellison syndrome ;
• (eradication of Helicobacter pylori ), including chronic (together with antibacterial drugs );
• relapses peptic ulcer caused by Helicobacter pylori .

Contraindications

Absolute contraindications for the drug are considered, as well as hypersensitivity to the components of the drug, usually to rabeprazole or substituted benzimidazole .

Side effects

When using the drug from the side Gastrointestinal tract, respiratory and nervous system , as well as musculoskeletal system the following side effects may occur:

• , decreased appetite, stomatitis, vomiting and nausea, dryness of the oral mucosa, increased activity of hepatic transaminases,;
• , asthenia, impaired vision and taste receptors,
  leukopenia, as well as thrombocytopenia;
• convulsions, myalgia, arthralgia;
• , cough and;
• back pain;
• an allergic reaction in the form of a rash.

Instructions for the use of Rabeprazole (Way and dosage)

Overdose

At the present time, there has been no scientifically confirmed data on the consequences of an overdose of the drug.

Interaction

You can use the drug in conjunction with , Theophylline, and, moreover, Phenytoin ... If medically necessary, the drug can be taken simultaneously with a proton pump inhibitor drug such as .

Terms of sale

Prescription.

Storage conditions

The drug should be kept out of the reach of children.

Best before date

special instructions

Before starting therapeutic treatment with Rabeprazole, the presence of malignant tumors in the digestive tract as the use of the drug can mask symptoms and complicate timely diagnosis oncological diseases .

With caution, the drug should be used in the presence of liver dysfunctions. With the simultaneous use of this drug, as well as and Ketonazole the dosage of the last two drugs should be adjusted.

If you experience such side effects of the drug as sleepiness and fatigue it is worth giving up driving or performing work that requires a high concentration of attention.