Hyrabezol pills 10mg, 15pcs

Composition

1 tablet contains:

Active ingredient:

rabeprazole sodium 10 mg;

Auxiliary substances:

magnesium oxide;

mannitol;

corn starch;

povidone K 30;

low-substituted hyprolose;

sodium stearyl fumarate;

Shell that is soluble in the intestine:

cellacephate; titanium dioxide; iron oxide red dye.

Pharmacological action

Pharmaceutical group:

reducing the secretion of gastric glands means-proton pump inhibitor.

Pharmaceutical action:

Hyrabezol is an anti-ulcer drug from the group of proton pump inhibitors (H+/K+-ATPASE), which is metabolized in the parietal cells of the stomach to active sulfonamide derivatives that inactivate the sulfhydryl groups of H+/K+ – ATPASE. Blocks the final stage of hydrochloric acid secretion, reducing the content of basal and stimulated secretion, regardless of the nature of the stimulus.

It has a high lipophilicity, easily penetrates the parietal cells of the stomach and concentrates in them, having a cytoprotective effect.

The antisecretory effect after oral use of 20 mg occurs within 1 hour and reaches a maximum in 2-4 hours; inhibition of basal and food – stimulated acid secretion 23 hours after the first intake is 62% and 82%, respectively; duration of action-48 hours. After the end of the reception, secretory activity normalizes within 2-3 days.

In the first 2-8 weeks of therapy, the concentration of gastrin in the blood serum increases and returns to baseline levels within 1-2 weeks after discontinuation of the drug. It does not affect the central nervous system, cardiovascular and respiratory systems.

Pharmacokinetics:

 Suction and distribution

It is absorbed from the small intestine (due to the presence of an acid-resistant enteric membrane). Absorption is high, the time to reach Cmax is 3.5 h. The values of Cmax and AUC are linear in the dose range from 10 to 40 mg. Bioavailability – 52%, does not increase with repeated use.

Binding to plasma proteins is 97%.

Metabolism and elimination

It is metabolized in the liver with the participation of cytochrome P 450 isoenzymes (CYP 2C19 and CYP 3A4).

T 1/2 – 0.7-1.5 h, clearance – 283 ± 98 ml/min. Excreted by the kidneys-90% in the form of two metabolites: a conjugate of mercapturic acid (M5) and carboxylic acid (M6); intestines – 10%.

Pharmacokinetics in special clinical cases

In patients with mild or moderate chronic hepatic insufficiency after a single dose, AUC increases by 2 times, T 1/2-by 2-3 times. After taking 20 mg of rabeprazole for 7 days, the AUC increases by 1.5 times, T 1/2-by 1.2 times. In patients with stable end-stage renal failure requiring hemodialysis (creatinine clearance less than 5 ml/min/1.73 m2), the distribution of rabeprazole sodium is close to that in healthy individuals.

In elderly patients, after taking rabeprazole for 7 days, the AUC is 2 times higher, the Cmax is 60% higher than in young patients. In patients with slow CYP2C19 metabolism, after 7 days of taking rabeprazole at a dose of 20 mg per day, AUC increases 1.9 times, and T1 / 2 increases 1.6 times compared to the same parameters in “fast metabolizers”, while Cmax increases by 40%.

Indications

• acute gastric and duodenal ulcer;
• gastroesophageal reflux disease;
• hypersecretory conditions, including Zollinger-Ellison syndrome;
• stress ulcers of the gastrointestinal tract.
• As part of complex therapy:
• eradication of Helicobacter pylori in patients with peptic ulcer of the stomach and duodenum or chronic gastritis;
• treatment and prevention of relapse of peptic ulcer associated with Helicobacter pylori.

Use during pregnancy and lactation

Rabeprazole should not be prescribed to pregnant women (there are no data on the safety of rabeprazole during pregnancy).

Breast-feeding should be discontinued for the duration of treatment.

It is not known whether rabeprazole is excreted in breast milk.

No relevant studies have been conducted in lactating women.

Contraindications

• pregnancy;
• breast-feeding;
• children and adolescents under 18 years of age;
• hypersensitivity to rabeprazole, benzimidazoles or other components of the drug.

With caution, the drug should be prescribed for severe hepatic insufficiency, severe renal insufficiency.

Side effects

• abdominal pain, nausea, loose stools or constipation
• headache, dizziness
• runny nose, cough
• decreased white blood cell count, blood platelet
• count allergic reactions.

Interaction

The drug Hyrabezol does not interact with liquid antacids.

In case of drowsiness, you should stop driving a car and other activities that require increased concentration of attention.

When taken together, preprat Hayrabezol reduces the effect.

How to take, course of use and dosage

Inside. Tablets should be swallowed whole, without chewing or grinding. It was found that neither the time of day nor food intake affect the activity of rabeprazole.

With acute gastric ulcer and anastomotic ulcer:  take 10 or 20 mg once a day. Usually, recovery occurs after 6 weeks of therapy, but in some cases, the duration of treatment can be extended by another 6 weeks.

In case of acute duodenal ulcer disease:  20 mg once a day. In some cases, the therapeutic effect occurs when taking 10 mg 1 time a day. The duration of treatment is from 2 to 4 weeks. If necessary, the duration of treatment can be extended by another 4 weeks.

In the treatment of erosive GERD or reflux esophagitis,10 or 20 mg once a day. The duration of treatment is from 4 to 8 weeks. If necessary, the duration of treatment can be extended by another 8 weeks.

With maintenance therapy of GERD,10 or 20 mg once a day. The duration of treatment depends on the patient’s condition.

For non-erosive GERD (GERD) without esophagitis, take 10 or 20 mg once a day.

If symptoms persist after 4 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 at a dose of 10 mg 1 time a day on request.

For the treatment of Zollinger-Allison 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 at a dose of up to 100 mg per day with a single dose or 60 mg 2 times a day. For some patients, fractional dosage of the drug is preferred. Treatment should be continued as clinically necessary. In some patients with Zollinger-Allison syndrome, the duration of treatment with rabeprazole is up to one year.

For the treatment of duodenal ulcer disease or chronic gastritis associated with H. pylori infection, a course of treatment lasting 7 days is recommended with one of the following drug combinations: :

• Hyrabezol 20 mg 2 times a day + clarithromycin 500 mg 2 times a day and amoxicillin 1 g 2 times a day.
• Hyrabezol 20 mg 2 times a day + clarithromycin 500 mg 2 times a day and metronidazole 400 mg 2 times a day.

Patients with renal and hepatic insufficiency. No dose adjustment is required in patients with renal insufficiency.

In patients with mild to moderate hepatic insufficiency, the concentration of rabeprazole in the blood is usually higher than in healthy patients.

Caution should be exercised when prescribing Hirabezol to patients with severe hepatic insufficiency.

Elderly patients. No dose adjustment is required.

Children. The safety and efficacy of rabeprazole 20 mg for short-term (up to 8 weeks) treatment of GERD in children aged 12 years and older is confirmed by extrapolating the results of adequate and well-controlled studies that support the effectiveness of rabeprazole for adults with safety and pharmacokinetics studies for children. The recommended dose for children aged 12 years and over is 20 mg once a day for up to 8 weeks. The safety and efficacy of rabeprazole for the treatment of GERD in children under 12 years of age has not been established. The safety and efficacy of rabeprazole for other indications has not been established for paediatric patients.

Overdose

Symptoms:  data on intentional or accidental overdose are minimal. There were no cases of severe overdose with rabeprazole.

Treatment:  the specific antidote for rabeprazole is unknown. Rabeprazole binds well to plasma proteins and is therefore poorly excreted during dialysis. In case of overdose, it is necessary to carry out symptomatic and supportive treatment.

Special instructions

The patient’s response to rabeprazole therapy does not exclude the presence of malignancies in the stomach. Hairabezol tablets should not be chewed or crushed. Tablets should be swallowed whole. It was found that neither the time of day nor food intake affect the activity of rabeprazole.

In a special study in patients with mild or moderate hepatic impairment, there was no significant difference in the frequency of side effects of rabeprazole from those in healthy individuals selected by gender and age, but despite this, caution is recommended when first prescribing rabeprazole to patients with severe hepatic impairment.

In patients with impaired renal or hepatic function, no dose adjustment is required. The AUC of rabeprazole in patients with severe hepatic impairment is approximately 2 times higher than in healthy patients.

Hypomagnesemia. When treated with proton pump inhibitors for at least 3 months, cases of symptomatic or asymptomatic hypomagnesemia have been reported in rare cases. In most cases, these reports were received one year after therapy. Serious adverse events included tetany, arrhythmia, and seizures. Most patients required treatment for hypomagnesemia, including magnesium replacement and discontinuation of proton pump inhibitor therapy. In patients who will be receiving long-term treatment or who are taking proton pump inhibitors with medications such as digoxin or medications that may cause hypomagnesemia (such as diuretics), healthcare professionals should monitor their magnesium levels before starting treatment with proton pump inhibitors and during treatment.

Fractures. According to observational studies, it can be assumed that therapy with proton pump inhibitors may lead to an increased risk of hip, wrist, and spine fractures associated with osteoporosis. The risk of fractures was increased in patients who took high doses of proton pump inhibitors for a year or more.

Form of production

Tablets

Storage conditions

Store in a dry place, protected from light, at a temperature of 8-25 °C

Shelf life

2 years

Active ingredient

Rabeprazole

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults by doctor’s prescription, Children by doctor’s prescription, Children over 12 years of age

Indications

for Reflux Esophagitis, Flatulence, Heartburn