HAIRABESOL PILLS 20MG

Composition:

Dosage 10 mg: Active ingredient: Rabeprazole sodium - 10 mg.

Excipients: Magnesium oxide 50 mg, mannitol 17.5 mg, corn starch 2.5 mg, povidon-K30 1.5 mg, low substituted hyprolosis 16 mg, sodium fumarate 2 mg.

Shell: cellulose phosphate 11.25 mg, titanium dioxide 1 mg, iron dye red oxide 0.1 mg.

Dosage 20 mg: Active ingredient: rabeprazole sodium - 20 mg.

Excipients: magnesium oxide 69 mg, mannitol 40 mg, corn starch 2.5 mg, povidon-K30 1.5 mg, low-substituted hyprolosis 24 mg, sodium fumarate 2 mg.

Shell: 18 mg cellulose, 1.6 mg titanium dioxide, iron dye yellow oxide 0.16 mg.

Description

Dosage 10 mg: round biconvex tablets, coated from light pink to reddish-pink color. In cross section, the core is white or white with a yellowish tinge.

Dosage 20 mg: round biconvex tablets, coated from light yellow to yellow color. In cross section, the core is white or white with a yellowish tinge.

Pharmacotherapeutic group: a means of reducing the secretion of the gastric glands - the proton pump inhibitor.

Pharmacological properties

Pharmacodynamics

Mechanism of action. Rabeprazole belongs to the class of antisecretory compounds, which are chemically substituted benzimidazoles.The drug inhibits the activity of the enzyme H + / K + -ATP-ase ("proton pump"), thereby blocking the final stage of the synthesis of hydrochloric acid. This effect is dose-dependent in nature and leads to inhibition of both basal and stimulated secretion of hydrochloric acid, regardless of the stimulus. As a weak base, rabeprazole in any doses is rapidly absorbed and concentrated in the acidic environment of the parietal cells.

Antisecretory activity. After ingestion of 20 mg of rabeprazole, an antisecretory effect occurs within one hour. The depression 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 the pharmacokinetic action far exceeds the predictable half-life (T1 / 2), which is approximately one hour. This effect can be explained by the binding of the drug substance to the H + / K + -ATPase of the parietal cells of the stomach. The magnitude of the inhibitory effect of rabeprazole sodium on acid secretion reaches a plateau after three days of taking rabeprazole sodium. When you stop taking secretory activity is restored within 1-2 days.

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

Effect on enterochromine-like cells. Studying the biopsy specimens of the bottom and antrum of the stomach in more than 500 patients who received rabeprazole sodium or a comparison drug lasting up to 8 weeks showed no changes in the morphological structure of enterochroma-phine-like (ECL) cells, the severity of gastritis, the frequency of atrophic gastritis, intestinal metaplasia or the prevalence of Helicobacter pylori

In a study involving more than 400 patients who received rabeprazole at a dose of 10 mg / day or 20 mg / day for up to 1 year, the frequency of hyperplasia was low and comparable to that for patients who received Omeprazole at a dose of 20 mg / day. Not a single case of adenomatous changes or carcinoid tumors was observed in rats.

Other effects. Currently, there is no evidence that rabeprazole causes systemic effects from the central nervous system (CNS), 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 also on the concentration in the blood of parathyroid hormone, Cortisone, estrogen, testosterone, prolactin, secretin, glucagon, follicle-stimulating hormone, luteinosis. renin, aldosterone and somatotropic hormone.

Pharmacokinetics

Absorption

Rabeprazole is rapidly absorbed from the intestine, and its peak plasma concentrations (Cmax) are reached approximately 3.5 hours after the 20 mg dose. Changes in peak plasma concentrations and area under the pharmacokinetic curve "concentration - time" (AUC) of rabeprazole are linear in the dose range from 10 to 40 mg. Absolute bioavailability after oral administration of 20 mg (compared with intravenous administration) is about 52%. In addition, the bioavailability does not change with repeated use of rabeprazole. Neither the time of the drug intake during the day, nor antacids affect the absorption of rabeprazole. Taking the drug with fatty foods slows down the absorption of rabeprazole for 4 hours or more, but neither Cmax nor the degree of absorption does not change.

Distribution

In humans, the degree of binding of rabeprazole with plasma proteins is about 97%. Metabolism

Rabeprazole is metabolized in the body in two ways. A significant part of it is metabolized in a systemic non-enzymatic way with the formation of thioether derivatives. Rabeprazole is also metabolized in the liver by cytochrome P450 to form sulfonic and desmethyl derivatives.

In healthy volunteers, the plasma half-life is about 1 hour (varies from 0.7 to 1.5 hours), and the total clearance is 3.8 ml / min / kg.

Removal

After a single oral dose of 20 mg of a 14C-labeled rabeprazole, about 90% of the drug is excreted in the urine, mainly in the form of carboxylic acid thioester, its glucuronide, and in the form of mercapturic acid derivatives. Unchanged drug in the urine is not determined.The remaining part of the taken rabeprazole is excreted through the intestines. The total elimination is 99.8%.

End-stage renal disease

In patients with stable renal failure in the terminal stage who need supporting hemodialysis (creatinine clearance <5ml / min / 1.73 m2), removal of rabeprazole is similar to that for healthy volunteers. The AUC and Cmax in these patients were approximately 35% lower than in healthy volunteers. On average, T1 / 2 rabeprazole was 0.82 hours in healthy volunteers, 0.95 hours in patients during hemodialysis, and 3.6 hours after hemodialysis. The clearance of the drug in patients with kidney disease in need of hemodialysis was approximately two times higher than in healthy volunteers.

Chronic compensated cirrhosis

Patients with chronic compensated cirrhosis of the liver tolerate rabeprazole well in a dose of 20 mg once a day, although the AUC is doubled and Cmax is increased by 50% compared with healthy volunteers.

Elderly patients

In elderly patients, the elimination of rabeprazole is somewhat delayed. After 7 days of taking rabeprazole in a dose of 20 mg 1 time per day in elderly people, the AUC was about twice as high, and Cmax increased by 60% compared with young healthy volunteers; no signs of drug cumulation were noted.

CYP2C19 polymorphism

In patients with delayed metabolism through the isoenzyme CYP2C19, after 7 days of taking rabeprazole at a dose of 20 mg per day, the AUC increases 1.9 times, and the half-life is 1.6 times compared to the same parameters in “fast metabolisers”, while as Cmax increases by 40%.

Indications for use

• Peptic ulcer of the stomach in the acute stage and ulcer of the anastomosis;
• Duodenal ulcer in the acute stage;
• Erosive and ulcerative gastroesophageal reflux disease or reflux esophagitis;
• Supportive 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 Helicobacter pylori eradication in patients with gastric ulcer and duodenal ulcer or chronic gastritis.

Contraindications

Hypersensitivity to rabeprazole, substituted benzimidazoles or other auxiliary components of the drug; pregnancy; breastfeeding period (lactation); children's age up to 12 years.

Carefully

Severe liver failure, severe renal failure, children age (over 12 years).

Use 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 caused by rabeprazole; however, in rats in small quantities, the drug penetrates the placental barrier. Rabeprazole should not be used during pregnancy except in cases where the expected positive effect on the mother exceeds the possible harm to the fetus. It is not known whether rabeprazole is excreted in breast milk.Relevant studies in nursing women have not been conducted. However, rabeprazole is found in the milk of lactating rats, so the drug cannot be used during breastfeeding.

Tablets drug Hairabesol can not be chewed or crushed. pills should be swallowed whole. It was established that neither the time of day nor food intake affect the activity of rabeprazole.

• In case of gastric ulcer in the acute stage and ulcer anastomosis It is recommended to take orally 20 mg once a day. Usually, the cure comes after 6 weeks of therapy, but in some cases the duration of treatment may be increased by 6 weeks.
• With duodenal ulcer in the acute stage It is recommended to take orally 20 mg once a day. The 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 (GERD) or reflux esophagitis It is recommended to take orally 20 mg once a day. The 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 of gastroesophageal reflux disease (GERD) It is recommended to take orally 10 mg or 20 mg once a day. The duration of treatment depends on the condition of the patient.
• In non-erosive gastroesophageal reflux disease (NERD) It is recommended to take orally 10 mg or 20 mg once a day.
• If after four weeks of treatment the symptoms do not disappear, additional research should be carried out on the patient. After stopping the symptoms to prevent their subsequent occurrence, the drug should be taken orally at a dose of 10 mg once a day as required.
• For the treatment of Zollinger-Elison syndrome and other conditions characterized by pathological hypersecretion, dose is selected individually. The initial dose is 60 mg per day, then the dose is increased and the drug is administered 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 of the drug is preferred. Treatment should continue as needed. In some patients with Zollinger-Alison syndrome, the duration of treatment with rabeprazole is up to one year.
• For eradication of Helicobacter pyloriIt is recommended to take orally 20 mg twice a day according to a specific scheme with the appropriate combination of antibiotics. The duration of treatment is 7 days.
• Patients with renal and hepatic failure
• Dose adjustment in 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.
• Caution should be exercised in prescribing Hairabesol in patients with severe hepatic insufficiency.
• Elderly patients
• Dose adjustment is not required.

Children

The safety and efficacy of rabeprazole in children aged 12 years and older has been established for short-term (up to 8 weeks) treatment of GERD. The recommended dose for children aged 12 years and older is 20 mg 1 time per day for up to 8 weeks. The safety and efficacy of rabeprazole for use in other indications has not been established for pediatric patients.

Side effect

Based on the experience of clinical studies, it can be concluded that rabeprozol is usually well tolerated by patients. The side effects are generally mild or moderate and are transient.

Undesirable reactions are systematized with respect to each of the organ systems using the following classification of the frequency of occurrence:

Very often (> 1/10)

Often (1/10 - 1/100)

Infrequently (1/100 - 1/1000)

Seldom (1/1000 - 1/10000)

Very rarely (<1/10000).

Immune system disorders: rarely, acute systemic allergic reactions.

Blood and lymphatic system disorders: rarely - thrombocytopenia, neutropenia, leukopenia.

Metabolic and nutritional disorders: rarely - hypomagnesemia.

Hepatobiliary system disorders: rarely - increased activity of “liver” enzymes, hepatitis, jaundice, hepatic encephalopathy.

Kidney and urinary tract disorders: very rarely - interstitial nephritis.

Violations of the skin and subcutaneous tissues: rarely - bullous rashes, urticaria, very rarely - erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome.

Disorders of the musculoskeletal and connective tissues: rarely - myalgia, arthralgia.

Disturbances from the reproductive system: very rarely - gynecomastia.

Changes in other laboratory parameters during the reception of rabeprazole sodium was not observed.

When taking proton pump inhibitors (PPIs), you may increase the risk of bone fractures (see "Special Instructions").

Overdose

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