Rezo - instructions for use, analogs, reviews and release forms (10 mg and 20 mg tablets) of the drug for the treatment of gastritis, stomach and duodenal ulcers, including Helicobacter in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Razo. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of specialists on the use of Razo in their practice. 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. Razo Analogues in the Presence of Available Structural Analogues.Use for the treatment of gastritis, stomach and duodenal ulcers, including Helicobacter in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Razo - antiulcer drug, inhibitor of H-K-ATPase (proton pump).

Mechanism of action

Rabeprazole (active ingredient in the preparation of Pazo) belongs to the class of antisecretory compounds, which are chemically substituted with benzimidazoles. The drug inhibits the activity of the enzyme H-K-ATPase (proton pump), thereby blocking the final stage of synthesis of hydrochloric acid. This effect is dose-dependent and leads to inhibition of both basal and stimulated secretion of hydrochloric acid regardless of the stimulus. As a weak base, Rabeprazole at any dose is rapidly absorbed and concentrated in the acidic environment of parietal cells.

Antisecretory activity

After ingestion of Pazo in a dose of 20 mg, the antisecretory effect develops within 1 hour. The oppression of basal and stimulated secretion of hydrochloric acid 23 hours after the first dose of rabeprazole sodium is 62% and 82% respectively and lasts up to 48 hours.This duration of pharmacokinetic action is much higher than the predicted half-life, which is about 1 hour. This effect can be explained by the binding of the drug substance to the HK-ATPase of parietal cells of the stomach. The magnitude of the inhibitory effect of rabeprazole sodium on acid secretion reaches a plateau after 3 days of taking rabeprazole sodium. At the termination of reception secretory activity is restored within 1-2 days.

Effect on the concentration of gastrin in serum

At the beginning of rabeprazole therapy, the concentration of gastrin in the serum increases, which is a reflection of the inhibitory effect on the secretion of hydrochloric acid. The concentration of gastrin returns to baseline usually within 1-2 weeks after discontinuation of treatment.

Effect on enterochromaffin-like cells

The study of biopsy specimens of the bottom and antrum of the stomach in more than 500 patients receiving rabeprazole sodium or a comparator for a duration of up to 8 weeks showed no changes in the morphological structure of enterochromaffin-like (ECL) cells, the degree of gastritis, the frequency of atrophic gastritis, intestinal metaplasia or the prevalence of infection, caused by Helicobacter pylori (Helicobacter).

In a study involving more than 400 patients receiving rabeprazole 10 mg / day or 20 mg / day for up to 1 year, the incidence of hyperplasia was low and comparable to that of patients treated with Omeprazole at a dose of 20 mg per day. There were no cases of adenomatous changes or carcinoid tumors observed in rats.

Other effects

At present, there is no evidence that rabeprazole causes systemic effects from the central nervous system, cardiovascular and respiratory systems. When administered orally at a dose of 20 mg for 2 weeks, rabeprazole had no effect on thyroid function, carbohydrate metabolism, and the concentration of parathyroid hormone, cortisol, estrogens, testosterone, prolactin, secretin, glucagon, FSH, LH, renin, aldosterone and growth hormone.

Composition

Rabeprazole sodium + excipients.

Pharmacokinetics

Rabeprazole is rapidly absorbed from the intestine. Absolute bioavailability after oral administration at a dose of 20 mg (compared with intravenous administration) is about 52%. In addition, bioavailability does not change with multiple administration of rabeprazole.Neither the time of taking the drug during the day, nor antacids affect the absorption of rabeprazole. The intake of the preparation with fatty food slows the absorption of rabeprazole by 4 hours or more, however, neither Cmax nor the degree of absorption is changed. The degree of binding of rabeprazole to plasma proteins is about 97%. Rabeprazole is metabolized in the body in two ways. A significant part of it is metabolized systemically non-enzymatically by formation of thioester derivatives. Rabeprazole is also metabolized in the liver via cytochrome P450 to form the sulfonic and desmethyl derivatives. After a single oral intake of 20 mg of 14C-labeled rabeprazole, about 90% of the drug is excreted in the urine, predominantly in the form of a thioester of a carboxylic acid, its glucuronide and as derivatives of mercapturic acid. Unchanged drug in urine is not determined. The rest of the accepted rabeprazole is excreted through the intestine. The total excretion is 99.8%.

In elderly patients, the elimination of rabeprazole is somewhat slowed down.

Indications

• stomach ulcer in the phase of exacerbation and ulcer of anastomosis;
• duodenal ulcer in the phase of exacerbation;
• erosive and ulcerative gastroesophageal reflux disease (GERD) or reflux esophagitis;
• maintenance therapy of gastroesophageal reflux disease;
• non-erosive gastroesophageal reflux disease;
• Zollinger-Ellison syndrome and other conditions characterized by pathological hypersecretion;
• as part of combination therapy to eradicate Helicobacter pylori in patients with peptic ulcer and duodenal ulcer or chronic gastritis.

Forms of release

Tablets coated with enteric coating 10 mg and 20 mg.

Instructions for use and reception scheme

The drug is taken orally. Tablets should be swallowed whole, without chewing or grinding. It has been established that neither the time of day nor the intake of food affects the activity of rabeprazole.

With peptic ulcer of the stomach in the phase of exacerbation and ulcer of the anastomosis, it is recommended to take 20 mg 1 time per day. Usually, the cure comes after 6 weeks of therapy, but in some cases the duration of treatment can be increased.

With duodenal ulcer in the acute phase, it is recommended to take 20 mg once a day.Duration of treatment is from 2 to 4 weeks. If necessary, the duration of treatment can be increased by another 4 weeks.

In the treatment of erosive gastroesophageal reflux disease or reflux esophagitis, it is recommended to take 20 mg 1 time per day. Duration of treatment is from 4 to 8 weeks. If necessary, the duration of treatment can be increased by another 8 weeks.

With maintenance therapy for gastroesophageal reflux disease, it is recommended to take 10 mg or 20 mg once a day 1 time per day. The duration of treatment depends on the patient's condition.

With non-erosive gastroesophageal reflux disease, it is recommended to take 10 mg or 20 mg once a day 1 time per day.

If after 4 weeks of treatment the symptoms do not disappear, an additional study of the patient should be carried out. After relief of symptoms to prevent their subsequent occurrence, the drug should be taken by mouth at a dose of 10 mg 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 once a day or 60 mg twice a day. For some patients, fractional dosing of the drug is preferred. Treatment should continue as clinical necessity. In some patients with Zollinger-Ellison syndrome, the duration of treatment with rabeprazole can be up to 1 year.

For eradication of Helicobacter pylori it is recommended to take inwards 20 mg twice a day according to a certain scheme with the appropriate combination of antibiotics. Duration of treatment is 7 days.

Correction of a dose to patients with renal insufficiency is not required.

In patients with mild and moderate hepatic insufficiency, the concentration of rabeprazole in the blood is usually higher than in healthy patients. Care should be taken when administering Razo to patients with severe hepatic impairment.

In elderly patients, dose adjustment is not required.

The safety and efficacy of rabeprazole in children aged 12 years and older is established for short-term (up to 8 weeks) treatment of GERD.The recommended dose for children aged 12 years and older is 20 mg once a day for up to 8 weeks. The safety and efficacy of rabeprazole for use in other indications is not established for pediatric patients.

Side effect

• headache;
• abdominal pain;
• diarrhea, constipation;
• flatulence;
• dry mouth;
• dizziness;
• rash;
• peripheral edema;
• acute systemic allergic reactions;
• thrombocytopenia, neutropenia, leukopenia;
• hypomagnesemia;
• increased activity of hepatic enzymes;
• hepatitis;
• jaundice;
• hepatic encephalopathy;
• interstitial nephritis;
• bullous eruptions;
• hives;
• erythema multiforme;
• toxic epidermal necrolysis;
• Stevens-Johnson syndrome;
• myalgia;
• arthralgia;
• gynecomastia.

When taking proton pump inhibitors, an increased risk of bone fractures may occur.

Contraindications

• pregnancy;
• the period of breastfeeding (lactation);
• children's age till 12 years;
• increased sensitivity to rabeprazole, substituted benzimidazoles or to the auxiliary components of the drug.

Application in pregnancy and lactation

There are no data on the safety of Razo's use during pregnancy. Studies of reproductive performance in rats and rabbits showed no signs of impaired fertility or fetal developmental defects caused by rabeprazole; However, in rats in small quantities, the drug penetrates the placental barrier. Rabeprazole should not be used during pregnancy, except when the expected positive effect on the mother exceeds the potential risk to the fetus.

It is not known whether rabeprazole is excreted in breast milk. Appropriate studies in lactating women were not conducted. However, rabeprazole is found in the milk of lactating rats, so the drug should not be used during breastfeeding.

Use in children

Contraindicated use of the drug in childhood to 12 years.

With caution should be prescribed in childhood (over 12 years).

Application in elderly patients

In elderly patients, dose adjustment is not required.

special instructions

The patient's response to rabeprazole sodium therapy does not exclude the presence of malignant neoplasms in the stomach.Before and after treatment, endoscopic control is necessary to exclude malignant neoplasm, because treatment with the drug can mask symptoms and delay correct diagnosis.

It is recommended to be careful when first prescribing the drug Razo to patients with severe impairment of liver function.

Patients with impaired renal or hepatic function are not required to adjust the dose of Razo. AUC of rabeprazole sodium in patients with severe impairment of liver function is approximately 2 times higher than in healthy patients.

The drug does not affect the function of the thyroid gland, the metabolism of carbohydrates, the concentration in the blood of parathyroid hormone, cortisol, estrogen, testosterone, prolactin, cholecystokinin, secretin, glucagon, FSH, LH, renin, aldosterone and somatotropic hormone.

According to observational studies, proton pump inhibitor therapy may lead to an increased risk of osteoporotic fractures of the hip, wrist, spine. The risk of fractures was increased in patients who received proton pump inhibitors in high doses for 1 year or more.

Impact on the ability to drive vehicles and manage mechanisms

Based on the peculiarities of pharmacodynamics of rabeprazole and its profile of undesirable effects, it is unlikely that the Razo drug affects the ability to drive vehicles and perform other activities requiring concentration of attention and speed of psychomotor reactions. However, in the case of drowsiness and dizziness, these activities should be avoided.

Drug Interactions

Rabeprazole does not enter into clinically significant interaction with Amoxicillin and other drugs metabolized by isoenzymes of the cytochrome P450 system in the liver: warfarin, phenytoin, theophylline and diazepam.

In connection with the fact that rabeprazole causes a pronounced and prolonged decline in the production of hydrochloric acid, there was an interaction with simultaneous reception with drugs, the absorption of which depends on the acidity of the contents of the stomach. In healthy volunteers, taking rabeprazole caused a decrease in the concentration of Ketoconazole in the blood plasma by 30% and an increase in Cmin Digoxin by 22%. With the simultaneous administration of rabeprazole with ketoconazole or digoxin, their doses should be adjusted.

With the simultaneous use of atazanavir 300 mg / ritonavir 100 mg with omeprazole (40 mg once a day) or atazanavir 400 mg with lansoprazole (60 mg once a day), a significant reduction in the effect of atazanavir was observed in healthy volunteers. Absorption of atazanavir depends on pH. Thus, simultaneous administration of atazanavir with proton pump inhibitors, including rabeprazole, is not recommended.

In the combined use of rabeprazole with clarithromycin, AUC and Cmax, in comparison with monotherapy, increased for rabeprazole by 11% and 34%, and for the active metabolite of Clarithromycin by 42% and 46%, respectively. This effect is used in the eradication of Helicobacter pylori.

Simultaneous administration of Razo and Methotrexate may lead to an increase in the concentration of methotrexate and its metabolite, hydroxymototrexate, and to increase the time of their elimination.

There was no clinically significant interaction of rabeprazole sodium with antacid preparations containing aluminum hydroxide or magnesium hydroxide.

There was no clinically significant interaction of rabeprazole with food.

Analogues of the drug Razo

Structural analogs for the active substance:

• Beret;
• Zulbeks;
• Нофлюкс;
• Ontime;
• Parries;
• Rabelock;
• Rabeprazole;
• Rabiet;
• Hyrabezole.

Analogues on the curative effect (remedies for the treatment of stomach and duodenal ulcers):

• Abisib;
• Acrylase;
• Almagel;
• Almagel Neo;
• Almol;
• Alfogel;
• Buscopan;
• Venter;
• Ventrisol;
• Vikair;
• Vikalin;
• Gastal;
• Ganaton;
• De Nol;
• Drotaverine;
• Zantak;
• Iberogast;
• Carolyn;
• Kwamatel;
• Controllers;
• Lanzap;
• Losek;
• Maalox;
• Methyluracil;
• Nexium;
• But the spine;
• Novobispol;
• Nolpaz;
• Octreotide;
• Omez;
• Omez Insta;
• Omeprazole;
• Omeface;
• Panavir;
• Pantoprazole;
• Papaverine;
• Pepsidine;
• Peptipack;
• Pepticum;
• Pylobakt AM;
• Platyphylline;
• Primamet;
• Ranigast;
• Ranitidine;
• Roxane;
• Spasmonet;
• Sulpiride;
• Talcid;
• Trimedate;
• Ulcozol;
• Ulkosan;
• Ulkavis;
• Ultop;
• Famosan;
• Famotidine;
• Phosphalugel;
• Hemomycin;
• Cimetidine;
• Cisagast;
• Eglonyl;
• Esomeprazole;
• Elenium;
• Emanera;
• Erbisol.

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