Khairabezol
Khairabezol: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Instructions for the use of Khairabezol: method and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews of Hayrabezole
- 19. Price of Khairabezol in pharmacies
Latin name: Hirabezol
ATX code: A02BC04
Active ingredient: Rabeprazole (Rabeprazole)
Manufacturer: HiGlance Laboratories Pvt. Ltd. (India)
Description and photo update: 2018-23-10
Khairabezol - proton pump inhibitor; a drug designed to lower the secretion of the gastric glands.
Release form and composition
Dosage form of the drug Khairabezol - tablets coated with a film enteric coating: round, biconvex, a white or white core with a yellowish tinge stands out at the fracture, the color of the shell depends on the dosage: 10 mg - from light pink to reddish pink; 20 mg - from light yellow to yellow (10, 14 or 15 pcs. In strips / blisters; in a cardboard box 1 or 10 strips / blisters of 10 pcs., 1, 2 or 10 strips / blisters of 14 or 15 pcs..; in a cardboard box, on the inside protected by PVC film, with perforations and a valve 1 strip / blister, 14 or 15 pcs.; 100, 500 or 1000 pcs. in polyethylene bags, in a high density polyethylene jar 1 bag - for hospitals).
Composition of Khairabezol tablets:
- active ingredient: sodium rabeprazole - 10 or 20 mg;
- excipients: mannitol, magnesium oxide, corn starch, low-substituted hyprolose, povidone-K30, sodium stearyl fumarate;
- enteric film shell: cellacephate, titanium dioxide; for a dosage of 10 mg, iron oxide red, for a dosage of 20 mg, iron oxide yellow.
Pharmacological properties
Pharmacodynamics
Khairabezol is a drug that has an antiulcer effect. The active substance in Khairabezol, rabeprazole, belongs to the group of proton pump inhibitors [hydrogen-potassium adenosine triphosphatase (H + / K + -ATP-ase)]. Its metabolism occurs in the parietal cells of the stomach, rabeprazole is cleaved to active derivatives of sulfonamide, inactivating sulfhydryl groups of H + / K + -ATPases. The blocking of the final stage of hydrochloric acid secretion occurs due to a decrease in the content of basal and stimulated secretion, regardless of the etiology of the stimulus.
Possessing high lipophilicity, rabeprazole easily penetrates into stomach cells that secrete hydrochloric acid and Castle's intrinsic factor, and concentrating in them has a cytoprotective effect.
After oral administration at a dose of 20 mg, the antisecretory effect occurs within 1 hour, reaching a maximum after 2–4 hours. Inhibition of acid secretion 23 hours after the first dose is: basal - 62%, stimulated food - 82%. The duration of action of the drug is 48 hours. The secretory activity is normalized after the end of the administration for 2-3 days.
At the beginning of treatment, for 2 to 8 weeks, the serum concentration of gastrin increases, its return to the initial levels occurs 1–2 weeks after stopping the intake of Hayrabesol. The drug has no effect on the cardiovascular, central nervous and respiratory systems.
Pharmacokinetics
Absorption of Khairabezol occurs in the small intestine (due to the presence of an acid-resistant enteric coating in the tablets). The absorption of rabeprazole is high, the time to reach the maximum plasma concentration (C max) is about 3.5 hours. The C max and area under the concentration-time curve (AUC) are linear. The bioavailability of the substance with repeated administration does not increase and is equal to 52%, up to 97% of rabeprazole binds to plasma proteins.
The metabolism of the drug is carried out in the liver with the participation of cytochrome P 450 (isoenzymes CYP 2C19 and CYP 3A4).
The half-life (T 1/2) is from 0.7 to 1.5 hours, the clearance value is 283 ± 98 ml / min. The main part of rabeprazole, up to 90%, is eliminated in the urine through the kidneys in the form of two metabolites [carboxylic acid (M6) and mercapturic acid conjugate (M5)], the remaining 10% is excreted in feces.
Pharmacokinetic characteristics in special clinical situations:
- chronic hepatic failure of mild or moderate degree: as a result of a single dose, the indicators increase: AUC - 2 times, T 1/2 - 2-3 times; as a result of taking 20 mg for 7 days, the growth of indicators is: for AUC - 1.5 times, for T 1/2 - 1.2 times;
- renal failure with creatinine clearance (CC) <5 ml / min / 1.73 m 2, in a stable terminal stage, requiring hemodialysis: the distribution of rabeprazole practically corresponds to that in healthy individuals;
- advanced age: as a result of taking rabeprazole for 7 days, the AUC indicator doubles, C max - by 60% in comparison with young patients;
- slow metabolism of cytochrome P 450 CYP2C19: as a result of taking rabeprazole for 7 days at a dose of 20 mg / day, the following indicators increase: AUC - 1.9 times, T 1/2 - 1.6 times in comparison with similar parameters in fast metabolizers, C max in this case increases by 40%.
Indications for use
According to the instructions, Khairabezol is recommended to be taken for the treatment of the following diseases:
- peptic ulcer of the duodenum and stomach in the acute stage;
- stress ulcers of the gastrointestinal tract (gastrointestinal tract);
- GERD (gastroesophageal reflux disease);
- pathological hypersecretory conditions, including Zollinger-Ellison syndrome.
In addition, Khairabezol is taken as part of the complex treatment of patients with gastric ulcer and duodenal ulcer or chronic gastritis for the eradication of Helicobacter pylori, as well as for the treatment and prevention of recurrence of peptic ulcer disease associated with this bacterium.
Contraindications
Absolute:
- the period of pregnancy and lactation (breastfeeding);
- children under 12 years old;
- hypersensitivity to substituted benzimidazoles, rabeprazole and / or auxiliary ingredients of the drug.
Relative (Khairabezol is taken with caution):
- severe renal / hepatic impairment;
- age from 12 to 18 years (for short-term treatment of GERD, for other indications the effectiveness and safety of the drug have not been established).
Instructions for the use of Khairabezol: method and dosage
Khairabezol tablets are taken orally, without crushing or chewing, swallowing whole to avoid disrupting the integrity of the film shell. The activity of rabeprazole does not depend on the time of day and food intake.
Recommended dosing regimen according to indications:
- peptic ulcer 12 duodenal ulcer / stomach in the acute stage: 20 mg 1 time per day, the course of therapy - from 4 to 6 weeks;
- GERD: treatment - 20 mg once a day, the course of therapy - from 4 to 8 weeks; maintenance treatment - 10 or 20 mg once a day, depending on the patient's response; symptomatic treatment in patients without esophagitis: 10 mg once a day for 4 weeks.
For the treatment of Zollinger-Ellison syndrome and other conditions characterized by pathological hypersecretion of gastric juice, the attending physician selects the dose individually.
Treatment of chronic gastritis resulting from infection with Helicobacter pylori, or peptic ulcer of the duodenum / stomach is recommended for a course of 1 week using one of the following combinations:
- I - 2 times a day: 20 mg Khairabezol + 500 mg clarithromycin + 1000 mg amoxicillin;
- II - 2 times a day: 20 mg Khairabezol + 500 mg clarithromycin + 400 mg metronidazole.
Side effects
- digestive system: often - nausea, diarrhea; infrequently - abdominal pain, constipation, vomiting, flatulence; rarely - belching, dry mouth, dyspepsia; extremely rare - stomatitis, dysgeusia, anorexia, gastritis, increased activity of liver enzymes;
- nervous system and sensory organs: often - headache; rarely - asthenia, dizziness, insomnia; extremely rarely - drowsiness, nervousness, depression, taste disturbance, visual impairment;
- musculoskeletal system: rarely - myalgia; extremely rare - cramps of the calf muscles, arthralgia;
- respiratory system: rarely - inflammation or infection of the upper respiratory tract, severe cough; extremely rare - bronchitis, sinusitis;
- hematopoietic organs and hemostasis system: rarely - leukopenia, thrombocytopenia; extremely rare - leukocytosis;
- allergic reactions: rarely - skin rash, itching of the skin;
- other reactions: rarely - pain in the chest, back, limbs, urinary tract infection, swelling, chills, fever, flu-like syndrome; extremely rare - hyperhidrosis, weight gain.
Overdose
The symptomatology of an overdose of Khairabezol has not been studied due to insufficient data on intentional or accidental excess of the recommended dosage. Rabeprazole 60 mg twice daily or 160 mg once caused minimal reversible side effects.
Rabeprazole does not have a specific antidote. Dialysis is ineffective because the drug binds well to plasma proteins, which significantly reduces its excretion. Symptomatic and supportive treatment is recommended.
special instructions
Before taking Khairabezol and at the end of the course of therapy, it is imperative to conduct endoscopic control in order to exclude malignant neoplasms, since treatment can mask the symptoms of the disease and delay the correct diagnosis.
Patients with severe hepatic disease should use caution when taking rabeprazole for the first time.
Khairabezol does not affect the metabolism of carbohydrates, the function of the thyroid gland, as well as the blood levels of cortisol, estrogen, parathyroid hormone, testosterone, prolactin, secretin, glucagon, cholecystokinin, luteinizing hormone, follicle-stimulating hormone, renin, somatotropic hormone.
Discontinuation of the drug does not cause withdrawal syndrome, secretory activity is restored due to the synthesis of new enzyme molecules within 2-3 days.
Influence on the ability to drive vehicles and complex mechanisms
If drowsiness develops during therapy, driving and performing other work requiring a high concentration of attention and speed of psychomotor reactions should be abandoned.
Application during pregnancy and lactation
There is insufficient data on the efficacy and safety of rabeprazole in pregnant and lactating women, therefore, Khairabezole should not be prescribed during pregnancy, and breastfeeding should be interrupted during therapy.
Pediatric use
In pediatric practice, rabeprazole is used for short-term (no more than 8 weeks) treatment of GERD in children and adolescents over 12 years old.
When used in patients under 18 years of age for other indications, the efficacy and safety of rabeprazole has not been established.
With impaired renal function
There is no need to adjust the dose of Khairabezol for patients with renal insufficiency.
For violations of liver function
Mild to moderate hepatic impairment can increase the plasma concentration of rabeprazole compared to that in healthy patients.
Severe hepatic impairment requires caution during therapy with Hayrabesol.
Use in the elderly
There is no need to adjust the dose of Khairabezol for elderly patients.
Drug interactions
- phenytoin, diazepam, indirect anticoagulants, some other drugs that are metabolized in the liver by microsomal oxidation: rabeprazole slows down their excretion;
- ketoconazole, digoxin: rabeprazole reduces their concentration by 33% and 22%, respectively;
- liquid antacids: no drug interaction with rabeprazole was noted;
- theophylline, warfarin, phenytoin, diazepam (drugs metabolized by the CYP 450 system): compatible with Khairabezol.
Analogs
The analogues of Khairabezol are: Noflux, Bereta, Zulbeks, Pariet, Razo, Rabelok, Ontime, etc.
Terms and conditions of storage
Keep out of the reach of children, in a dry place at temperatures up to 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Hayrabesol
Most reviews about Khairabezol speak of the rapid action of the drug, the state of health when it is taken improves practically on the second day of treatment, discomfort and pain in the stomach disappear. Many patients consider the ratio of efficiency and price to be optimal, indicating that there is no significant difference between the effect of taking Khairabezol and treatment with more expensive drugs.
Adverse reactions included minor headaches and constipation.
Price for Khairabezol in pharmacies
Estimated price for Khairabezol:
- tablets 10 mg: for 15 pcs. in the package - 364 rubles, for 30 pcs. in the package - 584 rubles;
- tablets 20 mg: for 15 pcs. in the package - 529 rubles, for 30 pcs. in the package - 769 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
