Khairabezol tablets p / o 20mg, No. 15
Expiration Date: 11/2025
Russian Pharmacy name:
Хайрабезол таблетки п/о 20мг, №15
peptic ulcer of the stomach and duodenum in the acute stage;
gastroesophageal reflux disease;
hypersecretory conditions, including Zollinger-Ellison syndrome;
stress ulcers of the gastrointestinal tract.
As part of complex therapy:
eradication of Helicobacter pylori in patients with gastric ulcer and duodenal ulcer or chronic gastritis;
treatment and prevention of recurrence of peptic ulcer disease associated with Helicobacter pylori.
The drug is prescribed at 20 mg 1 time / day. The tablets should be taken orally, in the morning before meals, swallowing whole, without chewing or crushing.
In case of duodenal ulcer and gastric ulcer in the acute stage, appoint 20 mg (1 tab.) 1 time / day in the morning for 4-6 weeks.
When gastroesophageal reflux disease (GERD) is prescribed 20 mg (1 tab.) 1 time / day for 4-8 weeks.
For maintenance therapy for GERD - at 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 - at 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 Helicobacter pylori infection, a 7-day course of treatment with one of the following drug combinations is recommended:
Khairabezol 20 mg 2 times / day + clarithromycin 500 mg 2 times / day and amoxicillin 1 g 2 times / day.
Khairabezole 20 mg 2 times / day + clarithromycin 500 mg 2 times / day and metronidazole 400 mg 2 times / day.
Active ingredient: sodium rabeprazole - 20 mg,
Excipients : magnesium oxide - 50 mg, mannitol - 17.5 mg, corn starch - 2.5 mg, povidone K30 - 1.5 mg, low-substituted hyprolose - 16 mg, sodium stearyl fumarate - 2 mg.
Shell composition: cellacephate - 11.25 mg, titanium dioxide - 1 mg, iron dye red oxide - 0.1 mg.
pregnancy;
breast-feeding;
children and adolescents up to 18 years old;
hypersensitivity to rabeprazole, benzimidazoles or other components of the drug.
The drug should be prescribed with caution in severe hepatic failure, severe renal failure.
Description:
Tablets, enteric-coated film coated from light yellow to yellow, round, biconvex; on a cross section, the core is white or white with a yellowish tinge.
Composition:
Active ingredient: sodium rabeprazole - 20 mg,
Excipients : magnesium oxide - 50 mg, mannitol - 17.5 mg, corn starch - 2.5 mg, povidone K30 - 1.5 mg, low-substituted hyprolose - 16 mg, sodium stearyl fumarate - 2 mg.
Shell composition: cellacephate - 11.25 mg, titanium dioxide - 1 mg, iron dye red oxide - 0.1 mg.
Clinical and pharmacological group: N + -K + -ATPase inhibitor. Antiulcer drug
Pharmaco-therapeutic group: Proton pump inhibitor
pharmachologic effect
An antiulcer drug from the group of proton pump inhibitors (H + / K + -ATP-ase), is metabolized in the parietal cells of the stomach to active sulfonamide derivatives that inactivate the sulfhydryl groups of H + / K + -ATP-ase.
Blocks the final stage of hydrochloric acid secretion, reducing the content of basal and stimulated secretion, regardless of the nature of the stimulus.
Possesses 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; inhibition of basal and food-stimulated acid secretion 23 hours after the first dose is 62% and 82%, respectively; duration of action - 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, serum gastrin concentration 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
Absorption and distribution
Absorbed from the small intestine (due to the presence of an acid-fast enteric membrane). Absorption is high, the time to reach Cmax is 3.5 hours. The Cmax and AUC values ??are linear in the dose range from 10 to 40 mg. Bioavailability - 52%, does not increase with repeated administration.
Communication with plasma proteins - 97%.
Metabolism and excretion
It is metabolized in the liver with the participation of cytochrome P450 isoenzymes (CYP 2C19 and CYP 3A4).
T1 / 2 - 0.7-1.5 h, clearance - 283 ± 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); intestines - 10%.
Pharmacokinetics in special clinical situations
In patients with mild or moderate chronic hepatic insufficiency, after a single dose, AUC doubles, T1 / 2 - 2-3 times. After taking 20 mg of rabeprazole for 7 days, AUC increases 1.5 times, T1 / 2 - 1.2 times. In patients with stable end-stage renal disease requiring hemodialysis (CC less than 5 ml / min / 1.73 m2), the distribution of rabeprazole sodium is close to that in healthy individuals.
In elderly patients, after taking rabeprazole for 7 days, the AUC is 2 times higher, Cmax is 60% more than in young people.
In patients with a slow metabolism of CYP2C19, after 7 days of taking rabeprazole at a dose of 20 mg per day, AUC increases 1.9 times, and T1 / 2 1.6 times compared with the same parameters in 'fast metabolizers', while Cmax increases by 40 %.
Indications
peptic ulcer of the stomach and duodenum in the acute stage;
gastroesophageal reflux disease;
hypersecretory conditions, including Zollinger-Ellison syndrome;
stress ulcers of the gastrointestinal tract.
As part of complex therapy:
eradication of Helicobacter pylori in patients with gastric ulcer and duodenal ulcer or chronic gastritis;
treatment and prevention of recurrence of peptic ulcer disease associated with Helicobacter pylori.
Dosage regimen
The drug is prescribed at 20 mg 1 time / day. The tablets should be taken orally, in the morning before meals, swallowing whole, without chewing or crushing.
In case of duodenal ulcer and gastric ulcer in the acute stage, appoint 20 mg (1 tab.) 1 time / day in the morning for 4-6 weeks.
When gastroesophageal reflux disease (GERD) is prescribed 20 mg (1 tab.) 1 time / day for 4-8 weeks.
For maintenance therapy for GERD - at 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 - at 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 Helicobacter pylori infection, a 7-day course of treatment with one of the following drug combinations is recommended:
Khairabezol 20 mg 2 times / day + clarithromycin 500 mg 2 times / day and amoxicillin 1 g 2 times / day.
Khairabezole 20 mg 2 times / day + clarithromycin 500 mg 2 times / day and metronidazole 400 mg 2 times / day.
Side effect
WHO classification of undesirable adverse reactions by 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 appointments (? 0.01%, but <0.1%), very rarely - less than 1/10 000 appointments (<0.01%).
From the digestive system: often - diarrhea, nausea; infrequently - vomiting, abdominal pain, flatulence, constipation; rarely - dry mouth, belching, dyspepsia; 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 disturbances, disturbances in taste.
From the musculoskeletal system: rarely - myalgia; very rarely - arthralgia, cramps of the calf muscles.
From the respiratory system: rarely - inflammation or infection of the upper respiratory tract, severe cough; very rarely - sinusitis, bronchitis.
From the side of the hematopoietic system and the hemostasis system: rarely - thrombocytopenia, leukopenia; very rarely - leukocytosis.
Allergic reactions: rarely - rash, itchy skin.
Others: rarely - pain in the back, chest, extremities, edema, urinary tract infection, fever, chills, flu-like syndrome; very rarely - increased sweating, weight gain.
Contraindications for use
pregnancy;
breast-feeding;
children and adolescents up to 18 years old;
hypersensitivity to rabeprazole, benzimidazoles or other components of the drug.
The drug should be prescribed with caution in severe hepatic failure, severe renal failure.
Application during pregnancy and lactation
Rabeprazole should not be administered during pregnancy (there is no data on the safety of rabeprazole during pregnancy).
It is not known whether rabeprazole is excreted in breast milk. Appropriate studies have not been conducted in lactating women. During treatment, breastfeeding should be discontinued.
Application for violations of liver function
The drug should be prescribed with caution in severe hepatic impairment.
No dose adjustment is required in patients with impaired liver function.
Application for impaired renal function
The drug should be prescribed with caution in severe renal failure.
No dose adjustment is required in patients with impaired renal function.
Application in children
The drug is not recommended for use in children, since there is no experience with the use of rabeprazole in pediatric practice.
Use in elderly patients
In elderly patients, after taking rabeprazole for 7 days, the AUC is 2 times higher, Cmax is 60% more than in young people.
special instructions
Before and after treatment with rabeprazole, endoscopic control is required to exclude malignant neoplasms. treatment can mask symptoms and delay correct diagnosis.
Caution is advised when first administering rabeprazole to patients with severely impaired 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 and somatotropic hormone.
No dose adjustment is required in patients with impaired renal or hepatic function.
Cancellation of the drug is not accompanied by the phenomenon of rebound, the restoration of secretory activity occurs within 2-3 days as new enzyme molecules are synthesized.
Use in pediatrics
The drug is not recommended for children and adolescents, since there is no experience with the use of rabeprazole in pediatric practice.
Influence on the ability to drive vehicles and use mechanisms
If drowsiness appears during treatment, you should abandon driving and other activities that require increased concentration of attention and speed of psychomotor reactions.
Overdose
Symptoms: not described.
Treatment: if an overdose is suspected, supportive and symptomatic therapy is recommended. Dialysis is ineffective.
Drug interactions
Rabeprazole slows down the excretion of some drugs that are 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).
Storage conditions
The drug should be stored in a dry, dark place, out of reach of children, at a temperature of 8 ? C to 25 ? C.
Shelf life
Shelf life is 2 years.
Terms of sale
The drug is available with a prescription.