Zulbex
Zulbeks: 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. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Zulbex
ATX code: A02BC04
Active ingredient: Rabeprazole (Rabeprazole)
Manufacturer: KRKA (Slovenia)
Description and photo update: 18.10.2018
Prices in pharmacies: from 400 rubles.
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Zulbex - proton pump inhibitor; an agent that lowers the secretion of stomach glands.
Release form and composition
Dosage form - enteric-coated tablets: round, convex on both sides, orange-pink (10 mg tablets) or brownish-yellow (20 mg tablets) color, 10 mg tablets - beveled (14 and 15 pcs. In blisters, 1, 2 or 4 blisters are packed in a cardboard box).
Composition of 1 tablet:
- active substance: rabeprazole sodium - 10 or 20 mg (which corresponds to the content of rabeprazole 9.42 and 18.85 mg, respectively);
- auxiliary components: hyprolosis, low-substituted hyprolose, mannitol (E421), light magnesium oxide;
- binder layer of the shell: light magnesium oxide, ethyl cellulose;
- enteric coating: talc, titanium dioxide (E171), diacetylated monoglycerides, hypromellose phthalate, iron dye yellow oxide (E172), iron dye red oxide (E172).
Pharmacological properties
Pharmacodynamics
Rabeprazole - a drug from the class of antisecretory agents, substituted benzimidazoles having no antihistamine (H 2) and cholinolytic properties and suppress gastric secretion by inhibiting proton pump (enzyme H + / K + -ATPase). The drug has a dose-dependent effect, suppresses basal and stimulated secretion of hydrochloric acid in the stomach, regardless of stimulating factors. According to animal studies, rabeprazole rapidly disappears from the gastric mucosa and blood plasma. Being a weak base, the substance in any dose is rapidly absorbed and accumulates in the acidic environment of the parietal cells of the stomach. Further, by protonation, it is converted into the sulfenamide form, after which it interacts with the available cysteine molecules of the proton pump.
The antisecretory effect of Zulbex develops within 1 hour after ingestion of 20 mg, reaching a maximum after 2–4 hours. 23 hours after taking the first dose, suppression of stimulated food and basal secretion of hydrochloric acid in the stomach is 82% and 69%, respectively, and lasts up to 48 hours. With regard to the secretion of hydrochloric acid, when taking repeated doses, the inhibitory effect of the drug increases slightly and reaches an equilibrium state after 3 days. After stopping the intake of rabeprazole, the secretory activity of the stomach is restored within 2-3 days.
According to in vitro studies, rabeprazole has a bactericidal effect on Helicobacter pylori bacteria. With its eradication by a combination of rabeprazole with antimicrobial drugs, a high degree of healing of mucosal lesions is noted. According to clinical studies, the use of rabeprazole at a dose of 20 mg 2 times a day simultaneously with two antibiotics (for example, metronidazole and clarithromycin or amoxicillin and clarithromycin) for 1 week in patients with gastroduodenal ulcers can eliminate H. pylori by more than 80% … When choosing the optimal combination in this case, it is necessary to be guided by the approved treatment standards. In the case of persistent infection (initially susceptible strains of microorganisms), when choosing a dosage regimen, the risk of developing secondary antibiotic resistance should be considered.
In clinical studies in patients who received 10 or 20 mg of rabeprazole 1 time per day for a period of up to 43 months, the concentration of serum gastrin in the first 2-8 weeks increased, reflecting the suppressive effect on the secretion of hydrochloric acid, with continued therapy, the concentration remained stable and returned to baseline values usually within 1–2 weeks after discontinuation of the drug.
Studies of fundus and antrum biopsies from more than 500 patients treated with rabeprazole or comparative treatment for up to 8 weeks showed no changes in histological and ECL cell structure, degree of gastritis, incidence of intestinal metaplasia or atrophic gastritis., the prevalence of H. pylori. More than 250 patients, who were followed up for 36 months of treatment, did not show significant changes in the initial conditions.
The systemic effects of rabeprazole on the cardiovascular, central nervous and respiratory systems have not been identified to date. When taking the drug at a dose of 20 mg for 2 weeks, no effect on the function of the thyroid gland, carbohydrate metabolism, circulating concentrations of growth hormone, aldosterone, follicle-stimulating hormone, renin, secretin, luteinizing hormone, testosterone, estrogen, prolactin, cortisol, glucagag cholecystokinin, parathyroid hormone.
Pharmacokinetics
Zulbex is available in the form of enteric-coated (i.e. stomach-stable) coated tablets, since rabeprazole is unstable in an acidic environment. Therefore, the absorption of the active substance begins in the intestine. C max (maximum concentration) of rabeprazole in plasma is reached 3.5 hours after ingestion of 20 mg. AUC (area under the concentration-time curve) and C maxare linear in the dose range from 10 mg to 40 mg. The absolute bioavailability of 20 mg of rabeprazole after oral administration is about 52% compared to intravenous administration. With repeated doses, bioavailability, presumably, does not increase. The half-life of the drug from blood plasma in healthy people is about 1 hour, the total clearance is 283 ± 98 ml / min. The time of taking the drug and food do not affect the absorption of rabeprazole.
The connection with blood plasma proteins is approximately 97%.
Rabeprazole is metabolized in the liver with the participation of CYP450 isoenzymes of cytochrome P 450. In in vitro studies, it was found that at the expected plasma concentrations in humans, the drug had no effect on CYP3A4, and this indicates the absence of interaction between rabeprazole and cyclosporine. The main metabolites found in plasma are carboxylic acid (M6) and thioester (M1); sulfonic acid (M2), desmethyl thioether (M4) and conjugate with mercapturic acid (M5) are determined in smaller amounts.
Approximately 90% of the taken dose of the drug is excreted by the kidneys in the form of two metabolites: carboxylic acid (M6) and conjugate with mercapturic acid (M5), as well as in the form of two unknown metabolites. The rest of the substance taken is found in the contents of the intestines.
There were no sex differences in the pharmacokinetic parameters of rabeprazole at a dose of 20 mg, taking into account adjustments for body weight and patient height.
In renal failure in patients on hemodialysis (creatinine clearance <5 ml / min / 1.73 m 2), the distribution of rabeprazole is similar to that in healthy volunteers, and C max and AUC are about 35% lower than these parameters in healthy people … The half-life of rabeprazole averages 0.82 hours in healthy volunteers, 0.95 hours in hemodialysis patients, and 3.6 hours after hemodialysis. The clearance of rabeprazole in hemodialysis patients due to functional impairment of the kidneys is approximately 2 times higher than in healthy people.
In mild and moderate liver dysfunctions, after a single dose of 20 mg of rabeprazole, AUC doubles, C max - 2-3 times compared with healthy volunteers, after regular intake of rabeprazole at a dose of 20 mg for 7 days, the AUC increases by 1, 5 times, C max - 1.2 times. Patient pharmacodynamic response (gastric pH control) is clinically comparable in both groups. The half-life for impaired liver function is 12.3 hours, while in healthy people it is 2.1 hours.
In elderly patients, the elimination of rabeprazole is somewhat slowed down. When taking the drug in a daily dose of 20 mg for 7 days, AUC increases by about 2 times, C max - by 60%, half-life - by 30%. There were no signs of drug accumulation.
In patients with a slow metabolism of CYP2C19 after taking 20 mg of rabeprazole, the AUC and the half-life are approximately 1.9 and 1.6 times higher than those in those with an active metabolism, while C max increases by 40%.
Indications for use
- Zollinger-Ellison syndrome;
- phase of exacerbation of gastric ulcer and 12 duodenal ulcer;
- gastroesophageal reflux disease (GERD): treatment of erosive reflux esophagitis and symptomatic therapy for GERD, including long-term maintenance;
- complex therapy for the eradication of Helicobacter pylori in gastric ulcer and duodenal ulcer or chronic gastritis;
- treatment and prevention of recurrence of peptic ulcer disease associated with H. pylori.
Contraindications
- hypersensitivity to any component of the drug;
- childhood;
- the period of pregnancy and breastfeeding.
According to the instructions, Zulbeks should be used with caution in severe renal failure.
Instructions for the use of Zulbeks: method and dosage
The tablets must be taken orally: swallowed whole with sufficient water. Do not crush or chew the tablets!
With exacerbation of peptic ulcer, 20 mg is prescribed 1 time per day, in the morning. Treatment of an active duodenal ulcer usually lasts 4 weeks, but some patients need to increase the course up to 8 weeks for complete healing of the ulcer; therapy of active benign gastric ulcer - 6 weeks, but some patients may need to increase the course up to 12 weeks.
With GERD, 20 mg is prescribed 1 time per day, the duration of therapy is 4-8 weeks. For long-term treatment, a maintenance dose of 10 or 20 mg can be used, depending on the individual effectiveness of therapy.
For the symptomatic treatment of GERD in patients without esophagitis, the recommended dose is 10 mg once a day. If within 4 weeks it is not possible to achieve control of the symptoms of the disease, an additional examination of the patient should be carried out. If the condition improves, symptoms can be controlled by taking Zulbex at a dose of 10 mg on demand.
In Zollinger-Ellison syndrome, the recommended starting dose is 60 mg once a day. If the effect is not enough, it is increased to 120 mg. A dose of up to 100 mg can be taken once a day, a dose of 120 mg should be divided into 2 doses of 60 mg each. The duration of treatment is determined by clinical indications.
For the eradication of Helicobacter pylori in patients with peptic ulcer disease or chronic gastritis, rabeprazole is prescribed in combination with antibiotics: Zulbex 20 mg 2 times a day, clarithromycin 500 mg 2 times a day, amoxicillin 1000 mg 2 times a day. If you need to take medications once a day, then Zulbex should be taken before breakfast. The course of treatment is 7 days.
Side effects
- from the nervous system: often (from> 1/100 to 1/1000 to 1/10 000 to <1/1000) - depression; very rarely (<1/10 000, including individual messages) - confusion;
- from the respiratory system: often - cough, rhinitis, pharyngitis; infrequently - sinusitis, bronchitis;
- from the musculoskeletal system: often - back pain, non-specific pain; infrequently - myalgia, arthralgia, calf muscle cramps;
- from the digestive system: often - abdominal pain, nausea, diarrhea, constipation, vomiting, flatulence; infrequently - dryness of the oral mucosa, dyspepsia, belching; rarely - change in taste, stomatitis, gastritis, jaundice, hepatitis, hepatic encephalopathy (in patients with concomitant cirrhosis of the liver);
- from the urinary system: infrequently - urinary tract infections; rarely - interstitial nephritis;
- on the part of the skin: infrequently - rash, erythema; rarely - bullous rash, sweating, itching; very rarely - Stevens-Johnson syndrome, erythema multiforme, toxic epidermal necrolysis;
- metabolic and nutritional disorders: rarely - weight gain or anorexia; very rarely - hyponatremia;
- on the part of the cardiovascular system: very rarely - peripheral edema;
- from the immune system: rarely - hypersensitivity reactions (including swelling of the face, shortness of breath, decreased blood pressure);
- on the part of the hematopoietic system: rarely - leukopenia, neutropenia, leukocytosis, thrombocytopenia;
- from the reproductive system: very rarely - gynecomastia;
- from the senses: rarely - visual disturbance;
- other: often - flu-like condition, asthenia;
- laboratory parameters: infrequently - increased activity of liver enzymes.
Overdose
Information about accidental or deliberate overdose is limited. It is known about cases of taking 60 mg of rabeprazole 2 times a day and 160 mg 1 time a day. The effects were insignificant, corresponded to the known spectrum of side effects and resolved on their own without medical intervention.
The specific antidote has not been established, and dialysis is ineffective. Treatment in case of overdose is symptomatic.
special instructions
Zulbex reduces the severity of symptoms, but this does not exclude the presence of malignant tumors in the stomach or esophagus. For this reason, before prescribing the drug, the patient is sent for examination in order to exclude neoplasms in the gastrointestinal tract.
With prolonged treatment (especially more than 1 year), patients should be examined regularly.
During the treatment period, there may be a change in the activity of liver enzymes, which passes after the drug is discontinued.
According to a post-marketing study, rabeprazole can cause the development of blood dyscrasias (thrombocytopenia, neutropenia). In most cases, when it was not possible to find out the alternative causes of such conditions, Zulbex was canceled, after which the dyscrasias passed without giving any complications.
The potential for cross-reactions with other proton pump inhibitors or substituted benzimidazoles should be considered.
Influence on the ability to drive vehicles and complex mechanisms
Given the properties of rabeprazole, the likelihood of its negative impact on the rate of reactions and attention is minimal. If side effects such as dizziness, drowsiness or confusion appear, it is recommended to refrain from driving and work that requires quick psychophysical reactions, as well as increased concentration of attention.
Application during pregnancy and lactation
In reproductive studies in rats and rabbits, signs of impaired fertility and the harmful effects of rabeprazole on the fetus were not detected, however, there are no data on the safety of taking the drug during pregnancy in humans, therefore Zulbex is contraindicated in women during this period of life.
In studies on rats, it was found that rabeprazole is secreted into milk. Studies in women have not been conducted, therefore, if necessary, a course of treatment during lactation is recommended to stop breastfeeding.
Pediatric use
Due to the lack of data on the safety of taking the drug in childhood, Zulbex is not used in pediatrics.
With impaired renal function
In case of impaired renal function, dose adjustment is not required.
In severe renal failure, the drug should be used with extreme caution.
For violations of liver function
In case of impaired liver function, there is no need to adjust the dose of Zulbex.
Drug interactions
Rabeprazole causes long-term and persistent suppression of the secretion of hydrochloric acid in the stomach, therefore it can interact with drugs, the degree of absorption of which depends on the pH values. With the simultaneous use of ketoconazole, a significant decrease in the concentration of both drugs in the blood plasma is possible, which requires dose adjustment.
Rabeprazole slows down the elimination of certain drugs metabolized in the liver by microsomal oxidation, such as indirect anticoagulants, diazepam and phenytoin.
Rabeprazole should not be taken in combination with atazanavir.
With the simultaneous use of Zulbex reduces the concentration of ketoconazole by 33%, and digoxin by 22%.
In the case of the combined use of rabeprazole with clarithromycin, an increase in the concentrations of both drugs is noted by 24% and 50%, respectively.
Analogs
Zulbeks analogs are: Pariet, Zolispan, Rabeprazole, Ontime, Rabeprazole-OBL, Vero-Rabeprazole, Khairabezol, Noflux.
Terms and conditions of storage
Keep out of reach of children at temperatures up to 30 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Zulbeks
Reviews about Zulbeks are mostly positive. This drug belongs to the new generation of rabeprazole inhibitors, which are more effective than those of lansoprazole and omeprazole. Zulbex is generally taken once a day, which patients find very convenient in everyday life.
Despite the fact that many took the drug for more than 1 month, there are practically no complaints about the development of pronounced side effects. The most common adverse reactions are constipation, bloating and headache.
Price for Zulbex in pharmacies
The price for Zulbex depends on the dosage and the number of tablets in the package:
- 14 tablets of 10 mg - 439-617 rubles;
- 14 tablets of 20 mg each - 470-1346 rubles;
- 28 tablets 10 mg each - 615-1020 rubles;
- 28 tablets, 20 mg each - 1337-1970 rubles.
Zulbeks: prices in online pharmacies
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Drug name Price Pharmacy |
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Zulbeks 20 mg enteric-coated tablets 14 pcs. RUB 400 Buy |
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Zulbeks tablets p.p. enteric solution. 20mg 14 pcs. RUB 537 Buy |
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Zulbeks 10 mg enteric-coated tablets 28 pcs. RUB 580 Buy |
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Zulbeks tablets p.p. enteric solution. 10mg 28 pcs. 586 r Buy |
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Zulbeks 20 mg enteric-coated tablets 28 pcs. 872 RUB Buy |
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Zulbeks tablets p.p. enteric solution. 20mg 28 pcs. RUB 879 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!
