Barol

General characteristics. Structure:

Active ingredient: 1 capsule contains a rabeprazol of sodium of 10 mg or 20 mg (in the form of kishechnorastvorimy pellets);

excipients: (structure of pellets) the neutral pellets (No. 16-18) covered magnesium with a carbonate, a gipromelloza, sodium hydroxide, magnesium a carbonate easy, the talc purified of methacrylic acid copolymer, a macrogoal, titanium dioxide (E171), ferrous oxide red (E172), ferrous oxide black (E172).

Pharmacological properties:

Pharmacodynamics.

Action mechanism. Rabeprazol belongs to a class of anti-secretory connections which in the chemical relation is the replaced benzim_dazola. Drug has no anticholinergic properties and H2 receptors are not an antagonist histamine, but suppress secretion of gastric acid by specific oppression of N+/K+-Atfazy enzyme on the secretory surface of covering cells of a stomach. This fermental system is considered the acid (proton) pump, and, thus, рабепразол is classified as inhibitor of the proton pump of a stomach that blocks a final stage of production of acid. Rabeprazol turns into an active sulfanam_dna a form by протонування and, thus, reacts with the available remains of cysteine of the proton pump.

Anti-secretory activity. After oral administration of a rabeprazol the anti-secretory effect is observed in an hour and reaches a maximum in 2 - 4 h. The effect of suppression of basal function and stimulation by food of secretion of acid in 23 h after reception of the first dose of a rabeprazol made 62 and 82% respectively, and duration of this effect reached 48 h. Efficiency of a rabeprazol in compliance acid secretion oppression amplifies a little in the course of daily reception of 1 tablet, but stable oppression of secretion is reached in 3 days after the beginning of reception of this drug. After completion of reception of a rabeprazol secretory activity within 2 - 3 days is normalized.

Influence on concentration of gastrin in serum. After reception of 10 or 20 mg of a rabeprazol of 1 times a day within 12 months in the first 2 - 8 weeks of therapy concentration of gastrin in serum increased that led to acid secretion oppression. Concentration of gastrin are returned to initial levels, as a rule, within 1-2 weeks after the treatment termination.

Other effects. Still there are no data about system effects from the central nervous system, cardiovascular and respiratory system which would be caused by reception of a rabeprazol.

Pharmacokinetics.

Absorption. Capsules, soluble in intestines, but not in a stomach. Absorption of a rabeprazol of sodium begins only after the capsule passes a stomach. Rabeprazol is quickly absorbed from intestines. Peak concentration of a rabeprazol in plasma are reached approximately in 3,5 h after reception in a dose of 20 mg. Peak concentration in plasma (Smakh) and the area under curve (AUC) of a rabeprazol have linear character in the range of doses from 10 to 40 mg. Absolute bioavailability after oral administration of 20 mg (in comparison with intravenous administration) makes about 52%, considerably - because of metabolism "the first passing. Besides, bioavailability at multiple dose of a rabeprazol does not increase. At healthy volunteers, plasma elimination half-life makes about an hour (from 0,7 to 1,5 h), and the total clearance is equal according to estimates of 283 minus 98 ml/min. The food and time of reception within a day do not influence absorption of a rabeprazol of sodium.

Distribution. Extent of linkng of a rabeprazol with proteins of plasma makes nearly 97%.

Metabolism and excretion. The main metabolites which are present at plasma is тіоефір (M1) and carboxylic acid (M6), and minor metabolites which are present at low concentration, presented by sulphone (Sq.m), dimetilt_oyeof_ry (M4) and a conjugate меркаптурово ї acid (M5). Insignificant anti-secretory activity has only a dimethyl metabolite (M3), however it is not present at plasma.

Indications to use:

Round ulcer of a duodenum, round ulcer of a stomach; gastroesophageal reflux disease (GERB); not ulcer dyspepsia; for Helicobacter pylori eradikation (N. pylor і) (in a combination with the appropriate antibacterial therapeutic means); Zollingera-Ellison's syndrome; chronic gastritis with raised acid-forming фукциею a stomach in an aggravation stage.

Route of administration and doses:

 At a round ulcer, a round ulcer of a stomach and GERB appoint to accept 20 mg 2 times a day. Duration of a course of treatment at a round ulcer of DPK makes 2 - 4 weeks, at stomach ulcer - 2 - 8 weeks, and at GERB - 4 - 8 weeks; the maintenance therapy at GERB makes 10 or 20 mg of 1 times a day up to 12 months.

At невиразковій dyspepsias appoint 40 mg of 1 times a day or on 20 mg two times a day within 2 - 3 weeks.

For N.'s eradikation of pylor_ it is necessary to address to schemes of complex therapy by the corresponding antibiotics (amoxicillin, klaritromitsiny, tetracycline), metronidazole, furasolidone and drugs of bismuth.

Barol on 20 mg 2 times a day + кларитромицин on 500 mg 2 times a day + amoxicillin on 1 g 2 times a day within 7 days.

Barol on 20 mg 2 times a day + кларитромицин on 500 mg 2 times a day + metronidazole on 500 mg 2 times a day within 7 days.

At Zollingera-Ellison's syndrome the initial dose makes 60 mg a day, if necessary the dose is raised to 120 mg a day (a daily dose of 80 mg and more it is necessary to divide into two receptions), the course of treatment and selection of a dose define individually.

At chronic gastritis with a stomach hyperoxemia in a stage of an aggravation appoint to accept 40 mg a day (on 1 capsule 2 times or 2 capsules of 1 times a day) within 2 - 3 weeks.

Capsules cannot be chewed or split up, it is necessary to swallow of them entirely.

Features of use:

Before use it is necessary to exclude existence at a sick malignant new growth.

At Barolu's appointment patients with heavy renal failures and a liver are recommended to be drug, careful at early stages of therapy.

It is not appointed for treatment of children as there is no experience of its use for patients of this age group.

Safety of use of Barolu during pregnancy is not studied. It is experimentally proved that drug can get through a placental barrier therefore its use during pregnancy is contraindicated. It is unknown, it is capable рабепразол to get into breast milk therefore Barol women who nurse should not appoint.

Considering an inherent profile of side effects of a rabeprazol, it is possible to consider that Barol should not influence negatively control of motor transport and work with potentially dangerous mechanisms. However in case of drowsiness it is recommended to abstain from driving and work with mechanisms.

In case of dermatological manifestations use of drug should be stopped.

Side effects:

 Of course Barol is well had by patients. Side effects which were observed were mostly insignificant, moderate and quickly passed. Diarrhea or a lock, an abdominal pain, nausea, vomiting, a meteorism, an eructation can be the most frequent negative manifestations from a digestive tract and a liver; seldom - increase in activity of liver enzymes, disturbance of flavoring feelings, dryness in a mouth.

From system of a hemopoiesis in some cases - a leukopenia, thrombocytopenia.

From a nervous system dizziness, a headache, excitement or drowsiness, a depression are possible.

Allergic reactions: skin rash, itch, Quincke's disease, bronchospasm.

Other manifestations: pharyngitis, a dorsodynia, a grippopodobny syndrome, a mialgiya, a stethalgia, sinusitis, spasms of gastrocnemius muscles, an infection of urinary tract, in isolated cases were observed increase in body weight, a vision disorder, the increased perspiration.

Interaction with other medicines:

Rabeprazol, as well as other inhibitors of the proton pump, is metabolized by enzymes which enter in hepatic system of P450 (CYP450) cytochrome. Rabeprazol causes strong and long decrease in production of gastric acid. Thus, рабепразол can interact with drugs which absorption depends on an indicator рН gastric contents. Reception of a rabeprazol causes decrease in concentration of a ketokonazol by 33% in a blood plasma and increase for 22% of the minimum concentration of digoxin. Thus, the certain patients using the specified drugs together with Barol have to be under observation of the doctor for definition of need for dose adjustment. The researches in vitro showed what рабепразол is metabolized by isoenzymes (CYP2C9 and CYP3A) of the CYP450 system. These researches allow to consider that Barol has low ability to interact with other drugs; at the same time its influence on cyclosporine metabolism similar influences of other inhibitors of the proton pump.

Contraindications:

Hypersensitivity to a rabeprazol, replaced benzimidazole or to any other ingredient of this drug. Pregnancy and lactation. Children's age.

Overdose:

Symptoms: the increased perspiration, dizziness, a headache, drowsiness, dryness in a mouth, nausea, vomiting.

Treatment: the specific antidote is not known. At overdose it is necessary to carry out the symptomatic and supporting treatment.

Storage conditions:

To store in the unavailable to children, dry, protected from light place at a temperature not above 25 °C. A period of validity - 2 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a strip; on 10 strips in cardboard packaging.