Rabelok tablets p / o 20mg, No. 14

• peptic ulcer of the stomach and duodenum in the acute phase

• peptic ulcer of the stomach and duodenum associated with Helicobacter pylori (in combination with antibiotics)

• gastroesophageal reflux.

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

It is taken internally. A single dose is 10-20 mg. The frequency and duration of use depend on the indications and treatment regimen.

Active ingredient: sodium rabeprazole - 20 mg

Excipients: mannitol - 89 mg, magnesium oxide - 80 mg, hypromellose - 5 mg, microcrystalline cellulose - 20 mg, starch - 20 mg, carmellose - 20 mg, talc - 3 mg, magnesium stearate - 6 mg, colloidal silicon dioxide - 3 mg.

Shell composition : hypromellose - 9.5 mg, propylene glycol - 1.5 mg.
The composition of the enteric shell: copolymer of methacrylic acid and ethyl acrylate (type C) (1: 1) - 13.95 mg, polysorbate 80 - 0.209 mg, dibutyl phthalate - 2.090 mg, sodium hydroxide - 0.119 mg, iron dye yellow oxide - 0.783 mg, talc - 5.63 mg, titanium dioxide - 1.210 mg.

• pregnancy,

• lactation period (breastfeeding)

• hypersensitivity to sodium rabeprazole or substituted benzimidazoles.

Description:

Enteric-coated tablets from light yellow to yellow, round, biconvex, smooth on both sides.

Composition:

Active ingredient: sodium rabeprazole - 20 mg

Excipients: mannitol - 89 mg, magnesium oxide - 80 mg, hypromellose - 5 mg, microcrystalline cellulose - 20 mg, starch - 20 mg, carmellose - 20 mg, talc - 3 mg, magnesium stearate - 6 mg, colloidal silicon dioxide - 3 mg.

Shell composition : hypromellose - 9.5 mg, propylene glycol - 1.5 mg.
The composition of the enteric shell: copolymer of methacrylic acid and ethyl acrylate (type C) (1: 1) - 13.95 mg, polysorbate 80 - 0.209 mg, dibutyl phthalate - 2.090 mg, sodium hydroxide - 0.119 mg, iron dye yellow oxide - 0.783 mg, talc - 5.63 mg, titanium dioxide - 1.210 mg.

Clinical and pharmacological group: N + -K + -ATPase inhibitor. Antiulcer drug

Pharmaco-therapeutic group: Proton pump inhibitor

pharmachologic effect

Antiulcer agent, inhibitor of H + -K + -ATPase (proton pump). The mechanism of action is associated with the inhibition of the enzyme H + -K + -ATPase in parietal cells of the stomach, which leads to blocking the final stage of the formation of hydrochloric acid. This action is dose-dependent and leads to inhibition of both basal and stimulated secretion of hydrochloric acid, regardless of the nature of the stimulus.

Pharmacokinetics

After oral administration, it is absorbed from the gastrointestinal tract. At a dose of 20 mg, Cmax is achieved after 3.5 hours. Changes in Cmax and AUC are linear (in the dose range from 10 to 40 mg). The absolute bioavailability is about 52% due to the 'first pass' effect through the liver. The bioavailability of rabeprazole does not increase with repeated administration.

Food intake and time of intake during the day do not affect the absorption of rabeprazole.

Plasma protein binding is 97%.

Rabeprazole sodium undergoes a 'first pass' effect. It is metabolized in the liver with the participation of isoenzymes of the CYP system.

Major metabolites (thioester and carboxylic acid) and minor metabolites (sulfone, dimethylthioester and mercaptopuric acid conjugate) are present at low concentrations.

In healthy volunteers, T1 / 2 is about 1 hour, the total clearance is about 283. Approximately 90% is excreted in the urine mainly in the form of two metabolites: a conjugate of mercaptopuric acid and carboxylic acid. In toxicological studies in laboratory animals, 2 more unidentified metabolites were found. The rest is excreted in the feces.

In patients with stable end-stage chronic renal failure requiring hemodialysis (CC less than 5 ml / min / 1.73 m2) AUC and Cmax were 35% lower than in healthy volunteers. On average, T1 / 2 of rabeprazole was 0.82 h in healthy volunteers, 0.95 h in patients during hemodialysis, and 3.6 h after hemodialysis. In renal diseases, the clearance of rabeprazole in hemodialysis patients was approximately 2 times higher than in healthy volunteers.

In patients with mild or moderate chronic hepatic failure, after a single dose of rabeprazole, an increase in Cmax, T1 / 2, AUC was observed.

In the case of a slow metabolism of CYP2C19 after taking rabeprazole at 20 mg / day for 7 days, AUC and T1 / 2 were 1.9 and 1.6, respectively, with extensive metabolism, while Cmax increased by only 40%.

In elderly patients, the elimination of rabeprazole is somewhat slowed down.

Indications

Ј Peptic ulcer and duodenal ulcer in the acute phase;

Х gastric ulcer and duodenal ulcer associated with Helicobacter pylori (in combination with antibiotics);

Ј Gastroesophageal reflux.

Dosage regimen

The method of application and dosage regimen of a particular drug depends on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly observe the compliance of the used dosage form of a particular drug with the indications for use and the dosage regimen.

It is taken internally. A single dose is 10-20 mg. The frequency and duration of use depend on the indications and treatment regimen.

Side effect

From the digestive system: diarrhea, nausea, abdominal pain, vomiting, flatulence, constipation; rarely - dry mouth, indigestion, belching; in isolated cases - anorexia, gastritis, stomatitis, increased activity of hepatic transaminases.

From the side of the central nervous system and peripheral nervous system: headache, asthenia, dizziness, insomnia; rarely - nervousness, drowsiness; in isolated cases - depression, impaired vision and taste.

From the respiratory system: possible - rhinitis, pharyngitis, cough; rarely - sinusitis, bronchitis.

Allergic reactions: rarely - skin rash; in isolated cases - itching.

Others: back pain, flu-like syndrome; rarely - myalgia, chest pain, chills, calf muscle cramps, urinary tract infection, arthralgia, fever; in isolated cases - an increase in body weight, increased sweating, leukocytosis.

Contraindications for use

Pregnancy, lactation (breastfeeding), hypersensitivity to sodium rabeprazole or substituted benzimidazoles.

Application during pregnancy and lactation

Rabeprazole is contraindicated during pregnancy and lactation.

In experimental studies , it was found that rabeprazole in small quantities penetrates the placental barrier, but there were no violations of fertility or fetal developmental defects; excreted in the milk of lactating rats.

There is no clinical experience with rabeprazole in children, so the use is not recommended.

Application for violations of liver function

Patients with impaired liver function do not require dose adjustment, but in patients with severely impaired liver function, rabeprazole is recommended to be used with caution.

Application for impaired renal function

No dose adjustment is required in patients with impaired renal function.

special instructions

Before starting therapy, it is necessary to exclude malignant neoplasms of the stomach, because the use of rabeprazole can mask symptoms and delay correct diagnosis.

Patients with impaired liver or kidney function do not require dose adjustment, however, in patients with severely impaired liver function, rabeprazole is recommended to be used with caution.

When used simultaneously with rabeprazole, the doses of ketoconazole and digoxin should be adjusted.

In experimental studies , the carcinogenic effect of rabeprazole has not been established, however, when studying mutagenicity, ambiguous results were obtained. Tests on lymphoma cells in mice were positive, with an in vivo micronucleus test and an in vivo and in vitro DNA repair test negative.

Drug interactions

With simultaneous use with digoxin, an increase (from small to moderate) in the concentration of digoxin in the blood plasma is possible.

When used simultaneously with ketoconazole, its bioavailability decreases.

Storage conditions

In a dry, dark place at a temperature not exceeding 25 ? C.

Keep out of the reach of children.

Shelf life is 2 years.

Conditions of dispensing from pharmacies

10 mg tablets - over the counter.

Tablets 20 mg - prescription.