Hyrabezol, 10 mg 15 pcs

Pharmgroup:

A gastric gland secretion reducing agent – proton pump inhibitor.

Pharmic action:

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

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

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

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

Pharmacokinetics:

Absorption and distribution

Absorbed from the small intestine (due to the presence of acid-resistant enteric coating). Absorption is high, time to reach Cmax – 3.5 h. Values of Cmax and AUC are linear in the dose range from 10 to 40 mg. Bioavailability is 52%, it does not increase with multiple administration.

The binding to plasma proteins is 97%.

Metabolism and excretion

Metabolized in liver with participation of cytochrome Р450 isoenzymes (CYP 2C19 and CYP 3A4).

T1/2 – 0.7-1.5 h, clearance – 283 ± 98 ml/min. Excreted by the kidneys – 90% as two metabolites: mercapturic acid conjugate (M5) and carboxylic acid (M6); by the intestines – 10%.

Pharmacokinetics in special clinical cases

In patients with mild to moderate chronic hepatic impairment after a single dose the AUC increases 2-fold, T1/2 – 2-3 times. After administration of 20 mg of rabeprazole during 7 days AUC is increased 1.5 times, T1/2 – 1.2 times. In patients with stable terminal renal failure requiring hemodialysis (CK less than 5 ml/min/1.73 m2), distribution of rabeprazole sodium is close to that in healthy subjects.

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

Indications

Active ingredient

Composition

1 tablet contains:

The active ingredient:

rabeprazole sodium10 mg;

Associates:

Magnesium oxide;

Mannitol;

Corn starch;

Povidon K30;

Hyprolose low-substituted;

Sodium stearyl fumarate;

Gut-soluble coating:

Cellacephate; titanium dioxide; red iron oxide dye.

How to take, the dosage

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

In acute peptic ulcer and anastomosis ulcer: 10 or 20 mg once daily. Usually cure occurs after 6 weeks of therapy, but in some cases the duration of treatment can be increased for another 6 weeks.

In acute duodenal ulcer: 20 mg once daily. In some cases the therapeutic effect occurs when taking 10 mg once a day. Treatment duration is from 2 to 4 weeks. If necessary, the duration of treatment may be increased for 4 more weeks.

In treatment of erosive GERD or reflux esophagitis 10 or 20 mg once daily. Duration of treatment is 4 to 8 weeks. If necessary, the duration of treatment may be increased for 8 more weeks.

In maintenance therapy of GERD 10 or 20 mg once daily. The duration of treatment depends on the patient’s condition.

In non-erosive GERD (NERD) without esophagitis, 10 or 20 mg once daily.

If symptoms do not disappear after 4 weeks of treatment, further investigation of the patient should be performed. After symptoms have resolved to prevent further onset, the drug should be taken orally at a dose of 10 mg once daily on demand.

To treat Zollinger-Elison syndrome and other conditions characterized by pathological hypersecretion, the dose is adjusted 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 at a single dose or 60 mg twice a day. For some patients, fractional dosing is preferable. Treatment should be continued as clinically necessary. In some patients with Zollinger-Elison syndrome, the duration of treatment with rabeprazole is up to one year.

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

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

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

Patients with severe hepatic impairment should use caution when prescribing Hyrabezole.

Elderly patients. No dose adjustment is necessary.

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 extrapolation of results of adequate and well-controlled studies supporting rabeprazole effectiveness for adults with safety and pharmacokinetic studies for pediatric patients. The recommended dose for children aged 12 years and older is 20 mg once daily for up to 8 weeks. Safety and efficacy of rabeprazole for GERD treatment in children less than 12 years old has not been established. Safety and efficacy of rabeprazole for other indications has not been established for pediatric patients.

Interaction

The drug Hyrabezole does not interact with liquid antacids.

In case of drowsiness it is necessary to refrain from driving and other activities requiring increased concentration.

When taken together, Hirabezole reduces the effect of .

Special Instructions

Patient response to therapy with rabeprazole does not exclude the presence of malignant neoplasms in the stomach. Hyrabezole tablets should not be chewed or crushed. The tablets should be swallowed whole. It has been found that neither time of day nor food intake affects the activity of rabeprazole.

In a special study in patients with mild to moderate liver dysfunction, no significant difference in the incidence of side effects of rabeprazole from that in gender- and age-matched healthy subjects was found, but despite this, caution is recommended when first prescribing rabeprazole to patients with severe liver dysfunction.

In patients with impaired renal or hepatic function, no adjustment of the dose of Hairabezole is necessary. 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 rarely been reported. Most of these cases were reported one year after therapy. Serious adverse events were tetany, arrhythmias, and seizures. Most patients required treatment for hypomagnesemia, which included magnesium replacement and discontinuation of proton pump inhibitor therapy. In patients who will receive long-term treatment or who take proton pump inhibitors with drugs such as digoxin or drugs that can cause hypomagnesemia (such as diuretics), health care providers should monitor magnesium levels before treatment with proton pump inhibitors and during treatment.

Fractures. Observational studies suggest that proton pump inhibitor therapy may lead to an increased risk of osteoporosis-related fractures of the hip, wrist, and spine. The risk of fractures has been increased in patients who have taken high-dose proton pump inhibitors for a year or more.

Contraindications

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

Side effects

Overdose

Symptoms: data on intentional or accidental overdose are minimal. No cases of severe overdose with rabeprazole have been reported.

Treatment: A specific antidote for rabeprazole is not known. Rabeprazole binds well to plasma proteins and is therefore poorly excreted by dialysis. In case of overdose, symptomatic and supportive treatment is necessary.

Pregnancy use

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

Breastfeeding should be stopped during treatment.

It is unknown whether rabeprazole is excreted with the breast milk.

No relevant studies have been performed in breastfeeding women.

Similarities