Razo
Razo: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application 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
- 19. Price in pharmacies
Latin name: Razo
ATX code: A02BC04
Active ingredient: Rabeprazole (Rabeprazole)
Manufacturer: Dr. Reddy's Laboratories Ltd. (India)
Description and photo update: 2018-23-10
Prices in pharmacies: from 211 rubles.
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Razo is an agent that lowers the secretion of stomach glands.
Release form and composition
Dosage form of release Razo - enteric-coated tablets: round, biconvex; 10 mg - from pink to brownish-pink, with black “RB10” marking on one side, 20 mg - from light yellow to yellow, with black “RB20” marking on one side; the cross section of the tablet shows an almost white core.
Packing of tablets: polymer cans with first opening control - 15 and 30 pcs., Blisters - 15 pcs., 1 can or 1-2 blisters are packed in a cardboard box.
Active ingredient: rabeprazole sodium, 1 tablet - 10 or 20 mg.
Additional components and their content in tablets (10/20 mg):
- excipients: mannitol - 48.505 / 97.01 mg, heavy magnesium oxide - 20/40 mg, low-substituted hyprolose - 7.2 / 14.4 mg, hypromellose 5 cps - 1.5 / 3 mg, magnesium stearate - 1.125 / 2, 25 mg, sodium lauryl sulfate - 0.9 / 1.8 mg, talc - 0.77 / 1.54 mg;
- shell: zein - 2.45 / 4.9 mg, triethyl citrate - 0.25 / 0.49 mg;
- enteric shell: methacrylic acid and ethyl acrylate copolymer [1: 1] (methacrylic acid copolymer, type C) - 12.05 / 19.28 mg, triethyl citrate - 1.2 / 1.92 mg, talc - 0.65 / 1, 04 mg.
Dye in the tablet shell:
- 10 mg: Opadrai pink O3B54475 - 2.7 mg (hypromellose 6 CP - 62.5%, macrogol-400 - 6.25%, titanium dioxide E171 - 28.7%, iron dye red oxide E172 - 2.55%;
- 20 mg: Opadry yellow OY-52945 - 5.05 mg (hypromellose 5 cP - 63.65%, macrogol-400 - 6.3%, titanium dioxide E171 - 28.55%, iron dye yellow oxide E172 - 1.5 %).
The composition of the ink used for the inscription on the tablets:
- 10 mg: isopropyl alcohol - 26.882%, propylene glycol - 2%, shellac glaze 45% - 44.467%, n-butanol - 2.242%, concentrated ammonia solution 28% - 1%, iron dye black oxide E172 - 23.409%;
- 20 mg: isopropyl alcohol - 3%, propylene glycol - 4%, shellac glaze 45% - 59%, n-butanol - 7%, concentrated ammonia solution 28% - 1%, titanium dioxide E171 - 5%, denatured ethanol - 6%, dye red charming E129 - 15%.
Pharmacological properties
Rabeprazole is a proton pump inhibitor; a substance that can lower the secretion of the stomach glands.
Pharmacodynamics
Mechanism of action
Rabeprazole belongs to the class of antisecretory compounds that are chemically substituted benzimidazoles. The substance inhibits the activity of the H + / K + -ATP-ase enzyme and thereby blocks the final stage of hydrochloric acid synthesis. This effect of the drug has a dose-dependent nature and, regardless of the stimulus, leads to inhibition of not only basal, but also stimulated secretion of hydrochloric acid. Being a weak base, regardless of doses, rabeprazole is rapidly absorbed and concentrated in the acidic environment of parietal cells.
Antisecretory activity
The antisecretory effect develops within 1 hour after taking the drug at a dose of 20 mg. 23 hours after taking the first dose, the inhibition of stimulated and basal secretion of hydrochloric acid is 82% and 62%, respectively. This pharmacological effect lasts up to 48 hours, which exceeds the expected parameters based on data on the half-life, by about 1 hour. The explanation for this effect is based on the long-term binding of rabeprazole to H + / K + -ATPase of gastric parietal cells. The inhibitory effect of the drug on the secretion of hydrochloric acid reaches its peak after 3 days of taking rabeprazole. After its cancellation, secretory activity is restored for 142 days.
Effect on enterochromaffin-like cells
Comparative studies were conducted in which more than 500 patients participated for a period of up to 8 weeks. Some received rabeprazole, others received a reference drug. According to the results based on the study of biopsies of the fundus and antrum of the stomach, there were no changes in the prevalence of Helicobacter pylori infection, the severity of gastritis, the morphological structure of enterochromaffin-like (ECL) cells, intestinal metaplasia and the frequency of atrophic gastritis.
In another study involving 400 patients who received rabeprazole at a daily dose of 10 or 20 mg for a period of up to 1 year, it was found that the incidence of hyperplasia did not differ from that of patients who received 20 mg of omeprazole per day. Also, not a single case of adenomatous changes or the development of carcinoid tumors observed in rats was recorded.
Effect on Serum Gastrin Concentration
At the initial stage of the use of rabeprazole, due to its inhibitory effect on the secretion of hydrochloric acid in the blood serum, the concentration of gastrin increases. It usually returns to baseline within 1–2 weeks after stopping therapy.
Other effects
When taking rabeprazole orally at a dose of 20 mg / day for 2 weeks, there was no negative effect on the metabolism of carbohydrates, the function of the thyroid gland, as well as the concentration in the blood of somatotropic hormone, luteinizing hormone, follicle-stimulating hormone, aldosterone, renin, estrogen, prolactin, testosterone, secretin, cortisol, glucagon, parathyroid hormone.
There is currently no evidence that the drug causes systemic effects from the central nervous, respiratory and cardiovascular systems.
Pharmacokinetics
Rabeprazole is highly absorbed. The maximum concentration (C max) reaches within 3.5 hours. Changes in C max and AUC (values of the area under the concentration-time curve) are linear in the dose range of 10–40 mg.
The drug is metabolized in the liver with the participation of CYP3A and CYP2C9 isoenzymes. Bioavailability after repeated administration does not increase and is 52%.
The connection with plasma proteins is 97%. The total clearance is 3.8 ml / min / kg. T1 / 2 (half-life) - 0.7-1.5 hours.
In patients with hepatic insufficiency, the AUC increases 2 times and T½ increases 2–3 times.
The time of taking the drug and antacids do not affect the absorption of rabeprazole. Fatty foods slow down its absorption by at least 4 hours, but the degree of absorption and maximum concentration do not change.
Excretion of rabeprazole: 10% - through the intestines, 90% - by the kidneys in the form of two metabolites: carboxylic acid (M6) and mercapturic acid conjugate (M5).
CYP2C19 polymorphism
In patients with a slow metabolism of CUR2C19, after a week of taking the drug in a daily dose of 20 mg, AUC increases 1.9 times, T½ by 1.6 times, and C max by 40%, when compared with the same parameters in patients who are "fast metabolizers ".
Elderly patients
Elderly people have a slightly slower elimination of rabeprazole. After a week of taking the drug in a daily dose of 20 mg in one dose, they have approximately 2 times increased AUC and 60% increased C max, when compared with healthy young volunteers.
No signs and symptoms of rabeprazole cumulation were noted.
Liver failure
Patients with chronic liver cirrhosis in the stage of decompensation tolerate rabeprazole at a daily dose of 20 mg well. However, in comparison with healthy volunteers, they have approximately 50% increased C max and 2 times - AUC.
Renal failure
With stable renal failure in the terminal stage (creatinine clearance <5 ml / min / 1.73 m 2) in patients requiring maintenance hemodialysis, the C max and AUC of rabeprazole are approximately 35% lower than in healthy volunteers, however, the excretion of the active substance Razo similar.
The clearance of the drug in patients with kidney disease who require hemodialysis is approximately 2 times higher than in healthy volunteers.
The half-life in healthy volunteers averaged 0.82 hours, in patients during hemodialysis - 0.95 hours, after hemodialysis - 3.6 hours.
Indications for use
- peptic ulcer of the duodenum in the acute stage;
- anastomotic ulcer;
- peptic ulcer in the acute stage;
- non-erosive gastroesophageal reflux disease;
- reflux esophagitis;
- peptic ulcer and erosive gastroesophageal reflux disease (including supportive therapy);
- Zollinger-Ellison syndrome;
- other conditions characterized by pathological hypersecretion.
Razo tablets are also used in combination therapy for chronic gastritis, gastric ulcer and 12 duodenal ulcer for the eradication of the Helicobacter pylori bacteria.
Contraindications
- age up to 12 years;
- pregnancy;
- period of breastfeeding;
- hypersensitivity to any component of the drug (both active and auxiliary) or other substituted benzimidazoles.
Razo should be used with caution when treating children over 12 years old, patients with severe renal / hepatic impairment.
Instructions for use of Razo: method and dosage
Razo is taken orally. The tablets should be swallowed whole, not crushed or chewed. Time of day and food intake do not have a clinically significant effect on the activity of rabeprazole.
The standard dosage of the drug Razo for various indications for adults:
- reflux esophagitis: 10 or 20 mg once a day. The duration of therapy is usually 4-8 weeks, in some cases it is increased to 12-16 weeks;
- anastomotic ulcer and exacerbation of gastric ulcer: 10 or 20 mg 1 time per day. The duration of therapy is usually 6 weeks, in some cases it is increased to 12 weeks;
- exacerbation of peptic ulcer of 12 duodenal ulcer: Razo 20 mg 1 time per day (in some patients, a daily dose of 10 mg may be effective). The course of therapy is 2–4 weeks, it can be increased to 6–8 weeks, if required;
- non-erosive gastroesophageal reflux disease: 10 or 20 mg 1 time per day. After relief of symptoms, treatment with the drug is continued in a daily dose of 10 mg in order to prevent relapse. If after 4 weeks of taking Razo, the symptoms of the disease do not disappear, additional research is required;
- eradication of Helicobacter pylori: 20 mg 2 times a day for 7 days as part of anti-Helicobacter pylori therapy (according to the scheme determined by the doctor);
- Zollinger-Ellison syndrome and other conditions with pathological hypersecretion: in an individual dose. At the beginning of therapy, 60 mg is usually prescribed 1 time per day, then, as a rule, the dose is increased by taking 100 mg 1 time per day or 60 mg 2 times a day (if a fractional dosage of Razo is more preferable). The duration of admission depends on the individual clinical need, the course can last up to 1 year;
- erosive gastroesophageal reflux disease (GERD): treatment - 10 or 20 mg 1 time per day for 4-8 weeks, in some cases, the course is increased to 12-16 weeks; maintenance therapy - 10 or 20 mg once a day, the duration of therapy is determined individually.
Children from 12 years old are prescribed Razo tablets only for GERD. The appropriate dose for their age is 20 mg once a day. In childhood, the drug can be used in a course of up to 8 weeks.
Side effects
Razo is usually well tolerated. Side effects, if any, are often mild to moderate and transient.
The following are the recorded adverse reactions classified by frequency of development as follows: very often -> 1/10, often - from 1/10 to 1/100, infrequently - from 1/100 to 1/1000, rarely - from 1/1000 to 1/10 000, very rarely - <1/10 000:
- instrumental and laboratory data: rarely - hypomagnesemia, leukocytosis, neutropenia, leukopenia, thrombocytopenia, increased activity of hepatic transaminases;
- skin and subcutaneous tissues: rarely - bullous rashes, urticaria, toxic epidermal necrolysis, Stevens-Johnson syndrome (severe erythema multiforme, characterized by the appearance of blisters and spots on the mucous membranes and skin, accompanied by high body temperature and joint pain);
- digestive system: often - dryness of the oral mucosa, abdominal pain, flatulence, diarrhea / constipation; rarely - jaundice, hepatitis; in patients with liver cirrhosis - hepatic encephalopathy;
- nervous system: infrequently - headache, dizziness;
- kidneys and urinary tract: very rarely - interstitial nephritis;
- musculoskeletal and connective tissue: rarely - myalgia, arthralgia;
- others: increased risk of bone fractures.
Overdose
There is practically no information about accidental or intentional overdose of Razo. There are known cases of taking the drug in a dose of 160 mg once or 60 mg 2 times a day. The side effects were minimal, reversible and did not require medical intervention.
There is no specific antidote to the drug. Rabeprazole binds well to plasma proteins, so it is poorly excreted during dialysis. Treatment of disorders due to overdose is symptomatic and supportive.
special instructions
Improvement of the patient's condition during therapy with Razo does not exclude the presence of malignant neoplasms in the stomach. Moreover, the drug can mask the symptoms, which makes timely diagnosis impossible. In this regard, before and after the end of treatment, endoscopic examination is necessarily indicated.
Observational studies have found that proton pump inhibitor therapy increases the risk of fractures of the wrist, hip and spine in patients with osteoporosis. People who receive these drugs in high doses for a long time (over 1 year) are more likely to have fractures.
Influence on the ability to drive vehicles and complex mechanisms
Based on data on the characteristics of the pharmacodynamics and the profile of side effects of rabeprazole, the possibility of a negative effect of Razo on the reaction rate and attention seems to be extremely low. However, patients in whom the drug causes dizziness and / or drowsiness should be abandoned during treatment from driving vehicles and working with complex mechanisms.
Application during pregnancy and lactation
There are no data on the safety / efficacy of rabeprazole during pregnancy. In reproductive studies carried out on rabbits and rats, no signs of impaired fertility and fetal developmental defects were found, but it was revealed that in rats the agent in small quantities penetrates the placental barrier. In this regard, Razo is not prescribed for pregnant women.
Whether rabeprazole is excreted in breast milk is unknown. Appropriate studies have not been conducted in lactating women. However, the drug was found in rat milk, so Razo is not prescribed for women who are breastfeeding.
Pediatric use
According to the instructions, Razo is contraindicated in patients under the age of 12 years.
In children over 12 years old, the safety and efficacy of using the drug only for short-term (up to 8 weeks) treatment of gastroesophageal reflux disease has been established. For other indications, Razo is not prescribed due to the lack of reliable data.
With impaired renal function
With caution, Razo should be used in severe renal failure. No dose adjustment is required.
For violations of liver function
Razo should be used with caution in severe hepatic insufficiency.
Patients with severely impaired liver function should be under medical supervision at the first administration of the drug. They have approximately 2 times higher AUC of rabeprazole compared to healthy volunteers, but dose adjustment is not required.
Use in the elderly
No dose adjustment of Razo is required for elderly patients.
Drug interactions
There were no clinically significant interaction reactions with the simultaneous use of Razo with food, liquid antacids, as well as amoxicillin and other drugs, if they are metabolized in the liver with the participation of cytochrome P 450 isoenzymes, such as warfarin, theophylline, diazepam and phenytoin.
With the combined use of rabeprazole and clarithromycin in the blood plasma, concentrations increase: by 24% - rabeprazole, by 50% - the active metabolite of clarithromycin. This effect is used in therapy aimed at eradication of the Helicobacter pylori bacteria.
Rabeprazole promotes a pronounced and long-term decrease in the production of hydrochloric acid, therefore it affects the action of drugs, the absorption of which depends on the acidity of the stomach contents. For example, in healthy volunteers, rabeprazole increased the minimum concentration of digoxin by 22% and decreased the plasma concentration of ketoconazole by 30%. In this regard, when prescribing such combinations, dose adjustment is required.
Razo increases the concentration of methotrexate and its active metabolite (hydroxymethotrexate), as well as increases the time of their excretion.
In healthy volunteers who received simultaneously 400 mg of atazanavir with lansoprazole at a dose of 60 mg once a day, or 300 mg of atazanavir / 100 mg of ritonavir with omeprazole at a dose of 40 mg once a day, a significant decrease in the effect of atazanavir, the absorption of which depends on pH … For this reason, atazanavir is not recommended for concomitant use with proton pump inhibitors, including rabeprazole.
Analogs
Razo's analogues are: Bereta, Zulbeks, Rabeprazol-SZ, Pariet, Khairabezol, Ontaym, Noflux, Rabelok.
Terms and conditions of storage
Store at a temperature not exceeding 25 ° C out of reach of children.
Shelf life of tablets in blisters is 3 years, in banks - 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Razo
There are few reviews about Razo on specialized medical forums. Patients confirm the effectiveness of the drug: it effectively eliminates pain and heaviness in the stomach, heartburn, lump in the throat, general weakness and other symptoms associated with pathological hypersecretion.
The disadvantages of the drug, many attribute the high cost compared to some other drugs containing rabeprazole as an active substance.
Price for Razo in pharmacies
The price for Razo is 305-350 rubles for 30 tablets in a dose of 10 mg, 385-475 rubles for 30 tablets of Razo 20 mg.
Razo: prices in online pharmacies
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Drug name Price Pharmacy |
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Razo tab. by. intestinal growth. 10 mg 15 pcs. 211 r Buy |
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Razo 10 mg enteric-coated tablets 15 pcs. 211 r Buy |
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One 10 mg enteric-coated tablets 30 pcs. 349 r Buy |
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Razo 20 mg enteric-coated tablets 30 pcs. 376 r Buy |
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!
