Expiration date: 01/2025
Product form, composition and packaging
Tablets coated with an intestinal-soluble shell from light yellow to yellow, round, biconvex, with a red marking "RB20" on one side, the cross-section of the core is almost white.
1 tablet - rabeprazole sodium 20 mg
Excipients: mannitol - 97.01 mg, low-substituted hyprolose - 14.4 mg, heavy magnesium oxide - 40 mg, hypromellose (5cps) - 3 mg, sodium lauryl sulfate - 1.8 mg, talc - 1.54 mg, magnesium stearate - 2.25 mg.
The composition of the inner shell: Zein - 4.9 mg, triethyl citrate - 0.49 mg.
Composition of the intestinal shell: methacrylic acid and ethylacrylate copolymer [1:1] - 19.28 mg, triethyl acetate - 1.92 mg, talc - 1.04 mg.
Composition of the outer shell: Opadray yellow OY-52945 - 5.05 mg, including hypromellose 6 cP - 63.65%, titanium dioxide - 28.55%, macrogol-400 - 6.3%, iron oxide yellow dye - 1.5%.
Red ink composition: shellac glaze - 59%, red charming dye - 15%, n-butanol - 7%, denatured ethanol - 6%, titanium dioxide - 5%, propylene glycol - 4%, isopropyl alcohol - 3%, concentrated ammonia solution - 1%.
15 PCs. - blisters (2) - packs of cardboard.
30 PCs. - banks polyethylene (1) - packs of cardboard.
Pharmacological action
Anti-ulcer agent, H+ - K+-ATPase (proton pump) inhibitor. The mechanism of action is associated with the inhibition of the H+-K+-ATPase enzyme in the parietal cells of the stomach, which leads to blocking the final stage of hydrochloric acid formation. This action is dose-dependent and leads to inhibition of both basal and stimulated hydrochloric acid secretion, regardless of the nature of the stimulus.
Pharmacokinetics
After ingestion, it is absorbed from the gastrointestinal tract. At a dose of 20 mg, Cmax is reached in 3.5 hours.changes in Cmax and AUC are linear (in the dose range from 10 to 40 mg). 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.
Binding to plasma proteins is 97%.
Rabeprazole sodium is subjected to the effect of "first pass". It is metabolized in the liver with the participation of CYP isoenzymes.
The main metabolites (thioester and carboxylic acid) and minor metabolites (sulfone, dimethylthioester and mercaptopuric acid conjugate) are present in low concentrations.
In healthy volunteers, T1/2 is about 1 h, the total clearance is about 283 Approximately 90% is excreted in the urine mainly in the form of two metabolites: mercaptopuric acid conjugate and carboxylic acid. In Toxicological studies, 2 more unidentified metabolites were found in laboratory animals. 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), the 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 kidney diseases, the clearance of rabeprazole in patients on hemodialysis was approximately 2 times higher than in healthy volunteers.
In patients with mild or moderate chronic liver failure after a single dose of rabeprazole, an increase in Cmax, T1/2, and AUC was observed.
In the case of delayed metabolism of CYP2C19 after taking rabeprazole 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 excretion of rabeprazole is somewhat slowed down.
Indications
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.
Dosage regimen
Take inside. 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, dyspepsia, belching, in some cases - anorexia, gastritis, stomatitis, increased activity of liver transaminases.
From the Central nervous system and peripheral nervous system: headache, asthenia, dizziness, insomnia, rarely - nervousness, drowsiness, in some cases - depression, visual disturbances and taste sensations.
From the respiratory system: possible - rhinitis, pharyngitis, cough, rarely - sinusitis, bronchitis.
Allergic reactions: rarely - skin rash, in some cases - itching.
Other: back pain, flu - like syndrome, rarely-myalgia, chest pain, chills, calf muscle cramps, urinary tract infection, arthralgia, fever, in some cases - weight gain, increased sweating, leukocytosis.
Contraindications to use
Pregnancy, lactation (breast-feeding), hypersensitivity to rabeprazole sodium or substituted benzimidazoles.
Use during pregnancy and lactation
Rabeprazole is contraindicated during pregnancy and lactation.
In experimental studies, it was found that rabeprazole in small amounts penetrates the placental barrier, but there were no violations of fertility or fetal development defects, it is excreted in the milk of lactating rats.
There is no clinical experience with rabeprazole in children, so it is not recommended.
Drug interaction
When used simultaneously with digoxin, it is possible to increase (from small to moderate) the concentration of digoxin in the blood plasma.
When used simultaneously with ketoconazole, its bioavailability decreases.
Application for violations of liver function
Patients with impaired liver function do not need to adjust the dose, but in patients with severe hepatic impairment, rabeprazole is recommended to be used with caution.
Use in cases of impaired renal function
Patients with impaired renal function do not need to adjust the dose.
Special instruction
Before starting therapy, it is necessary to exclude malignant neoplasms of the stomach, since the use of rabeprazole can mask the symptoms and delay the correct diagnosis.
Patients with impaired liver or kidney function do not need to adjust the dose, but in patients with severe hepatic impairment, rabeprazole is recommended to be used with caution.
When used simultaneously with rabeprazole, the dose of ketoconazole and digoxin should be adjusted.
Experimental studies have not established the carcinogenic effect of rabeprazole, but the study of mutagenicity has received mixed results. Tests on lymphoma cells in mice were positive, while the in vivo micronucleus test and the in vivo and in vitro DNA repair test were negative.
