Hayrabezol

General characteristics. Structure:

Active ingredient: 10 mg or 20 mg of a rabeprazol of sodium.

Excipients: magnesium oxide, Mannitolum, starch corn, K30 povidone, the hypro rod low-replaced the sodium stearylfumarating.

Structure of a cover: целлацефат, titanium dioxide, dye ferrous oxide red.

Antiulcerous drug.

Pharmacological properties:

Pharmacodynamics. Antiulcerous drug from group of inhibitors of the protonew pump (N + / To +-ATF-azy), is metabolized in covering cells of a stomach to active sulphonamide derivatives which inactivate the H+/K sulphhydryl groups +-ATF-azy.

Blocks a final stage of secretion of Acidum hydrochloricum, reducing the content of basal and stimulated secretion, irrespective of the irritant nature.

Has high lipophilicity, easily gets into covering cells of a stomach and concentrates in them, having cytoprotective effect.

The anti-secretory effect after oral administration of 20 mg occurs during 1 h and reaches a maximum in 2-4 h; oppression by basal and stimulated food of secretion of acid in 23 h after the first reception makes 62% and 82% respectively; action duration - 48 h. After the end of reception secretory activity is normalized within 2-3 days.

Concentration of gastrin in blood serum increases and returned to the first 2-8 weeks of therapy to initial levels within 1-2 weeks after drug withdrawal. Does not influence TsNS, cardiovascular and respiratory systems.

Pharmacokinetics. Absorption and distribution. It is absorbed from a small intestine (because of existence of an acid resisting kishechnorastvorimy cover). Absorption is high, time of achievement of Cmax - 3.5 h. Cmax and AUC values have linear character in the range of doses from 10 to 40 mg. Bioavailability - 52%, does not increase at multiple dose.

Communication with proteins of plasma - 97%.

Metabolism and removal. It is metabolized in a liver with participation of isoenzymes of P450 cytochrome (CYP 2C19 and CYP 3A4). T1/2 - 0.7-1.5 h, clearance - 283 ± 98 ml/min. It is removed by kidneys - 90% in the form of two metabolites: conjugate of mercapturic acid (M5) and carboxylic acid (M6); intestines - 10%.

Pharmacokinetics in special clinical cases. At patients with a chronic liver failure of weak or average degree after a single dose of AUC T1/2 - by 2-3 times increases twice. After reception of 20 mg of a rabeprazol within 7 days of AUC T1/2 - by 1.2 times increases by 1.5 time. At the patients with a stable end-stage of a renal failure needing a hemodialysis (KK less than 5 ml/min. / 1.73 sq.m), distribution of a rabeprazol of sodium is close to that at healthy faces.

At elderly patients after reception of a rabeprazol within 7 days of AUC is twice more, Cmax - is 60% more, than at young people.

At patients with the slowed-down metabolism of CYP2C19 after 7 days of reception of a rabeprazol in a dose of 20 mg in days of AUC T1/2 by 1.6 times in comparison with the same parameters at "bystry metabolizator" while Cmax increases by 40% increases by 1.9 times, and.

Indications to use:

— a peptic ulcer of a stomach and duodenum in an aggravation stage;

— gastroesophageal reflux disease;

— hyper secretory states, including Zollingera-Ellison's syndrome;

— stressful ulcers of a GIT.

As a part of complex therapy:

— Helicobacter pylori eradikation at patients with a peptic ulcer of a stomach and duodenum or chronic gastritis;

— treatment and prevention of a recurrence of the peptic ulcer connected with Helicobacter pylori.

Route of administration and doses:

Drug is appointed on 20 mg of 1 times/days. A pill should be taken inside, in the morning before meal, swallowing entirely, not chewing and without crushing.

At a peptic ulcer of a duodenum and a peptic ulcer of a stomach in a stage of an aggravation appoint 20 mg (1 таб.) 1 times/days in the morning within 4-6 weeks.

At a gastroesophageal reflux disease (GERB) appoint 20 mg (1 таб.) 1 times/days within 4-8 weeks.

For a maintenance therapy at GERB - in a dose of 10 or 20 mg of 1 times/days depending on the answer of the patient.

For a symptomatic treatment of GERB at patients without esophagitis - in a dose of 10 mg of 1 times/days within 4 weeks.

For the treatment of a syndrome of Zollingera-Ellison and other states which are characterized by pathological hypersecretion, the dose is selected individually.

For the treatment of a peptic ulcer of a duodenum or chronic gastritis connected with infection of Helicobacter pylori the course of treatment lasting 7 days of one of the following combinations of drugs is recommended:

Hayrabezol on 20 mg of 2 times/days + кларитромицин on 500 mg of 2 times/days and amoxicillin on 1 g 2 times/days.

Hayrabezol on 20 mg of 2 times/days + кларитромицин on 500 mg of 2 times/days and metronidazole on 400 mg of 2 times/days.

Features of use:

Use at pregnancy and feeding by a breast. Rabeprazol it is not necessary to appoint at pregnancy (there are no data on safety of use of a rabeprazol at pregnancy).

It is unknown whether it is allocated рабепразол with breast milk. The corresponding researches at the feeding women were not conducted. For the period of treatment it is necessary to stop breastfeeding.

Use at abnormal liver functions. With care it is necessary to appoint drug at a heavy liver failure.

Dose adjustment is not required to patients with abnormal liver functions.

Use at renal failures. With care it is necessary to appoint drug at a heavy renal failure.

Dose adjustment is not required to patients with renal failures.

Use for children. Children as there is no experience of use of a rabeprazol in pediatric practice are not recommended to appoint drug.

Use for elderly patients. At elderly patients after reception of a rabeprazol within 7 days of AUC is twice more, Cmax - is 60% more, than at young people.

Special instructions. Before treatment rabeprazoly endoscopic control for an exception of a malignant new growth since treatment can mask symptomatology is obligatory and delay the correct diagnosis.

It is recommended to be careful at the first purpose of a rabeprazol to patients with heavy abnormal liver functions.

Drug does not exert impact on function of a thyroid gland, metabolism of carbohydrates, on concentration in blood of parathyroid hormone, cortisol, estrogen, testosterone, prolactin, cholecystokinin, secretin, a glucagon, follicle-stimulating hormone, lyuteniziruyushchy hormone, a renin, Aldosteronum and somatotropic hormone.

Or a liver dose adjustment is not required to patients with renal failures.

Drug withdrawal is not followed by a ricochet phenomenon, recovery of secretory activity happens within 2-3 days in process of synthesis of new molecules of enzyme.

Use in pediatrics. Children and teenagers as there is no experience of use of a rabeprazol in pediatric practice are not recommended to appoint drug.

Influence on ability to driving of motor transport and to control of mechanisms. In case of emergence in the course of treatment of drowsiness it is necessary to refuse driving and other types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

The WHO classification of undesirable side reactions on development frequency: very often - 1/10 appointments (≥ 10%), are frequent - 1/100 appointments (≥ 1%, but <10%), infrequently - 1/1000 appointments (≥ 0.1%, but <1%), is rare - 1/10 000 appointments (≥ 0.01%, but <0.1%), is very rare - less than 1/10 000 appointments (<0.01%).

From the alimentary system: often - diarrhea, nausea; infrequently - vomiting, an abdominal pain, a meteorism, a lock; seldom - dryness in a mouth, an eructation, dyspepsia; very seldom - disturbance of flavoring feelings, anorexia, stomatitis, gastritis, increase in activity of transaminases.

From a nervous system and sense bodys: often - a headache; seldom - dizziness, an adynamy, sleeplessness; very seldom - nervousness, drowsiness, a depression, vision disorders, disturbances of flavoring feelings.

From a musculoskeletal system: seldom - a mialgiya; very seldom - an arthralgia, spasms of gastrocnemius muscles.

From respiratory system: seldom - an inflammation or an upper respiratory tract infection, a severe cough; very seldom — sinusitis, bronchitis.

From bodies of a hemopoiesis and system of a hemostasis: seldom - thrombocytopenia, a leukopenia; very seldom - a leukocytosis.

Allergic reactions: seldom — rash, a skin itch.

Others: seldom - a dorsodynia, breasts, extremities, hypostases, an infection of urinary tract, fever, a fever, a grippopodobny syndrome; very seldom - the increased perspiration, increase in body weight.

Interaction with other medicines:

Rabeprazol slows down removal of some medicines which are metabolized in a liver by a microsomal oxidation (diazepam, Phenytoinum, indirect anticoagulants).

Reduces concentration of a ketokonazol by 33%, digoxin - for 22%.

Does not interact with liquid antacids.

Let's combine with the drugs which are metabolized the CYP 450 system (warfarin, Phenytoinum, theophylline, diazepam).

Contraindications:

— pregnancy;

— breastfeeding;

— children's and teenage age up to 18 years;

— hypersensitivity to a rabeprazol, benzimidazoles or other components of drug.

With care it is necessary to appoint drug at a heavy liver failure, a heavy renal failure.

Overdose:

Symptoms: are not described.

Treatment: at suspicion on overdose the supporting and symptomatic therapy is recommended. Dialysis is inefficient.

Storage conditions:

Drug should be stored in dry, protected from light, the place, unavailable to children, at a temperature from 8 °C to 25 °C. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

10 pieces - blisters (1) - packs cardboard.
10 pieces - blisters (10) - packs cardboard.
10 pieces - strips (1) - packs cardboard.
10 pieces - strips (10) - packs cardboard.
14 pieces - blisters (1) - packs cardboard.
14 pieces - blisters (2) - packs cardboard.
14 pieces - strips (1) - packs cardboard.
14 pieces - strips (2) - packs cardboard.
15 pieces - blisters (1) - packs cardboard.
15 pieces - blisters (2) - packs cardboard.
15 pieces - blisters (10) - packs cardboard.
15 pieces - strips (1) - packs cardboard.
15 pieces - strips (2) - packs cardboard.
15 pieces - strips (10) - packs cardboard.