Composition, form of production and packaging
Tablets covered with enteric film coating from light pink to reddish-pink, round, biconvex; on the cross-section the nucleus is white or white with a yellowish tint of color.
1 tab.
rabeprazole sodium 10 mg
Excipients: magnesium oxide - 50 mg, mannitol - 17.5 mg, corn starch - 2.5 mg, povidone K30 - 1.5 mg, low-substituted giprolose - 16 mg, sodium stearyl fumarate - 2 mg.
The composition of the coating: cellacephate - 11.25 mg, titanium dioxide - 1 mg, iron oxide red oxide - 0.1 mg.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
10 pieces. - Strips (1) - packs of cardboard.
10 pieces. - Strips (10) - packs of cardboard.
14 pcs. - blisters (1) - packs of cardboard.
14 pcs. - blisters (2) - packs of cardboard.
14 pcs. - Strips (1) - packs of cardboard.
14 pcs. - Strips (2) - packs of cardboard.
15 pcs. - blisters (1) - packs of cardboard.
15 pcs. - blisters (2) - packs of cardboard.
15 pcs. - blisters (10) - packs of cardboard.
15 pcs. - Strips (1) - packs of cardboard.
15 pcs. - Strips (2) - packs of cardboard.
15 pcs. - Strips (10) - packs of cardboard.
Tablets, covered with an enteric film coating of the film from light yellow to yellow, round, biconcave; on the cross-section the nucleus is white or white with a yellowish tint of color.
1 tab.
rabeprazole sodium 20 mg
Excipients: magnesium oxide - 69 mg, mannitol - 40 mg, corn starch - 2.5 mg, povidone K30 - 1.5 mg, low-substituted giprolose - 24 mg, sodium stearyl fumarate - 2 mg.
The composition of the shell: tselatsefat - 18 mg, titanium dioxide - 1.6 mg, iron oxide oxide yellow - 0.16 mg.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
10 pieces. - Strips (1) - packs of cardboard.
10 pieces. - Strips (10) - packs of cardboard.
14 pcs. - blisters (1) - packs of cardboard.
14 pcs. - blisters (2) - packs of cardboard.
14 pcs. - Strips (1) - packs of cardboard.
14 pcs. - Strips (2) - packs of cardboard.
15 pcs. - blisters (1) - packs of cardboard.
15 pcs. - blisters (2) - packs of cardboard.
15 pcs. - blisters (10) - packs of cardboard.
15 pcs. - Strips (1) - packs of cardboard.
15 pcs. - Strips (2) - packs of cardboard.
15 pcs. - Strips (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2013.
PHARMACHOLOGIC EFFECT
An anti-ulcer drug from the proton pump inhibitor group (H + / K + -ATPase) is metabolized in parietal gastric cells to active sulfonamide derivatives that inactivate the sulfhydryl groups of H + / K + -ATPase.
It blocks the final stage of the secretion of hydrochloric acid, reducing the content of basal and stimulated secretion, regardless of the nature of the stimulus.
It has a high lipophilicity, easily penetrates into the parietal cells of the stomach and concentrates in them, providing a cytoprotective effect.
The antisecretory effect after oral administration of 20 mg occurs within 1 hour and reaches a maximum after 2-4 hours; depression of basal and stimulated food of acid secretion through 23 hours after the first intake is 62% and 82%, respectively; the duration of action is 48 hours. After the end of the reception, the secretory activity is normalized within 2-3 days.
In the first 2-8 weeks of therapy, the concentration of gastrin in the blood serum increases and returns to baseline levels within 1-2 weeks after drug withdrawal. Does not affect the central nervous system, cardiovascular and respiratory systems.
PHARMACOKINETICS
Suction and distribution
Absorbed from the small intestine (due to the presence of an acid-resistant enteric-soluble coat). Absorption is high, the time to reach C max is 3.5 h. The C max and AUC values ​​are linear in the dose range of 10 to 40 mg. Bioavailability - 52%, does not increase with multiple admission.
The connection with plasma proteins is 97%.
Metabolism and excretion
Metabolised in the liver with the participation of cytochrome P450 isoenzymes (CYP 2C19 and CYP 3A4).
T 1/2 - 0.7-1.5 h, clearance - 283 В± 98 ml / min. It is excreted by the kidneys - 90% in the form of two metabolites: a conjugate of mercapturic acid (M5) and carboxylic acid (M6); intestine - 10%.
Pharmacokinetics in special clinical cases
In patients with chronic hepatic insufficiency of mild or moderate degree after a single dose, the AUC increases 2 times, T 1/2 - 2-3 times. After taking 20 mg of rabeprazole for 7 days, the AUC increases 1.5 times, T 1/2 - 1.2 times. In patients with stable terminal stage of renal failure requiring hemodialysis (CC less than 5 ml / min / 1.73 m 2 ), the distribution of rabeprazole sodium is close to that in healthy individuals.
In elderly patients after taking rabeprazole for 7 days, AUC is 2 times greater, C max is 60% higher than in young patients.
In patients with delayed metabolism of CYP2C19 after 7 days of taking rabeprazole at a dose of 20 mg per day, the AUC increases 1.9 times, and T 1/2 by 1.6 times compared with the same parameters in "fast metabolizers," while C max increases on 40%.
INDICATIONS
- Stomach ulcer and duodenal ulcer in the stage of exacerbation;
- gastroesophageal reflux disease;
- hypersecretory conditions, including Zollinger-Ellison syndrome;
- Stress ulcers of the digestive tract.
As part of complex therapy:
- eradication of Helicobacter pylori in patients with peptic ulcer of stomach and duodenum or chronic gastritis;
- Treatment and prevention of recurrence of peptic ulcer associated with Helicobacter pylori.
DOSING MODE
The drug is prescribed 20 mg once a day. Tablets should be taken orally, in the morning before meals, swallowing whole, without chewing or grinding.
With peptic ulcer of duodenum and peptic ulcer of stomach at the stage of exacerbation appoint 20 mg (1 tab.) 1 time / day in the morning for 4-6 weeks.
In gastroesophageal reflux disease (GERD) , 20 mg (1 tab.) Are prescribed 1 time / day for 4-8 weeks.
For maintenance therapy with GERD - in a dose of 10 or 20 mg 1 time / day, depending on the patient's response.
For symptomatic treatment of GERD in patients without esophagitis - in a dose of 10 mg 1 time / day for 4 weeks.
For the treatment of Zollinger-Ellison syndrome and other conditions characterized by pathological hypersecretion, the dose is selected individually.
For the treatment of duodenal ulcer or chronic gastritis associated with infection with Helicobacter pylori, a course of treatment of 7 days with one of the following combinations of drugs is recommended:
Khayrabezol 20 mg 2 times / day + clarithromycin 500 mg 2 times / day and amoxicillin 1 g 2 times / day.
Hirabezol 20 mg 2 times / day + clarithromycin 500 mg 2 times / day and metronidazole 400 mg 2 times / day.
SIDE EFFECT
WHO classification of unwanted adverse reactions according to the frequency of development: very often - 1/10 appointments (? 10%), often - 1/100 appointments (? 1%, but <10%), infrequently - 1/1000 appointments (? 0.1% but <1%), rarely - 1/10 000 prescriptions (? 0.01%, but <0.1%), very rarely - less than 1/10 000 prescriptions (<0.01%).
From the digestive system: often - diarrhea, nausea; infrequently - vomiting, abdominal pain, flatulence, constipation; rarely - dry mouth, belching, indigestion; very rarely - a violation of taste, anorexia, stomatitis, gastritis, increased activity of transaminases.
From the nervous system and sensory organs: often - headache; rarely - dizziness, asthenia, insomnia; very rarely - nervousness, drowsiness, depression, visual impairment, taste disorders.
From the musculoskeletal system: rarely - myalgia; very rarely - arthralgia, spasms of the calf muscles.
On the part of the respiratory system: rarely - inflammation or infection of the upper respiratory tract, severe cough; very rarely - sinusitis, bronchitis.
On the part of the organs of hematopoiesis and hemostasis system: rarely - thrombocytopenia, leukopenia; very rarely - leukocytosis.
Allergic reactions: rarely - rash, itchy skin.
Other: rarely - pain in the back, chest, limbs, swelling, urinary tract infection, fever, chills, flu-like syndrome; very rarely - excessive sweating, weight gain.
CONTRAINDICATIONS
- Pregnancy;
- breast-feeding;
- children and adolescence under 18;
- hypersensitivity to rabeprazole, benzimidazoles or other components of the drug.
With caution should prescribe the drug in severe hepatic insufficiency, severe renal failure.
PREGNANCY AND LACTATION
Rabeprazole should not be prescribed during pregnancy (there is no safety data for the use of rabeprazole during pregnancy).
It is not known whether rabeprazole is excreted in breast milk. Appropriate studies in lactating women were not conducted. For the duration of treatment, breastfeeding should be discontinued.
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution should prescribe the drug in severe kidney failure.
Patients with impaired renal function do not need dose adjustment.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should prescribe the drug in severe hepatic insufficiency.
Patients with violations of the function of the liver dose adjustment is not required.
APPLICATION FOR CHILDREN
The drug is not recommended for children, since there is no experience of using rabeprazole in pediatric practice.
APPLICATION IN ELDERLY PATIENTS
In elderly patients after taking rabeprazole for 7 days, AUC is 2 times greater, C max is 60% higher than in young patients.
SPECIAL INSTRUCTIONS
Before and after treatment with rabeprazole, endoscopic control is necessary to exclude malignant neoplasm. treatment can mask symptoms and delay correct diagnosis.
It is advisable to use caution in the first appointment of rabeprazole to patients with severe impairment of liver function.
The drug does not affect the function of the thyroid gland, the metabolism of carbohydrates, the concentration in the blood of parathyroid hormone, cortisol, estrogen, testosterone, prolactin, cholecystokinin, secretin, glucagon, follicle stimulating hormone, luteinizing hormone, renin, aldosterone and somatotropic hormone.
Patients with impaired renal or hepatic function do not need a dose adjustment.
Abolition of the drug is not accompanied by a rebound phenomenon, the recovery of secretory activity occurs within 2-3 days as synthesis of new enzyme molecules.
Use in Pediatrics
The drug is not recommended for children and adolescents, since there is no experience of using rabeprazole in pediatric practice.
Impact on the ability to drive vehicles and manage mechanisms
In the case of the appearance of drowsiness during the treatment should be abandoned from driving and other activities that require increased concentration and speed of psychomotor reactions.
OVERDOSE
Symptoms: not described.
Treatment: if suspected overdose, supportive and symptomatic therapy is recommended. Dialysis is ineffective.
DRUG INTERACTION
Rabeprazole slows the excretion of certain drugs metabolized in the liver by microsomal oxidation (diazepam, phenytoin, indirect anticoagulants).
Reduces the concentration of ketoconazole by 33%, digoxin by 22%.
Does not interact with liquid antacids.
Compatible with drugs metabolized by the CYP 450 system (warfarin, phenytoin, theophylline, diazepam).
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, protected from light, out of reach of children at a temperature of 8 В° C to 25 В° C. Shelf life - 2 years.
