Rabeprazole-SZ
Rabeprazole-SZ: 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: Rabeprazole-SZ
ATX code: A02BC04
Active ingredient: rabeprazole (Rabeprazole)
Manufacturer: Severnaya Zvezda, CJSC (Russia)
Description and photo updated: 30.11.2018
Prices in pharmacies: from 92 rubles.
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Rabeprazole-SZ is a drug with antiulcer, anti-stress, proton pump inhibiting action.
Release form and composition
Dosage form - enteric capsules: hard gelatinous; dosage 10 mg - size No. 3, body color white, caps - dark red; dosage 20 mg - size No. 1, body color yellow, caps - brown; the contents of the capsules are spherical pellets from white with a yellowish or creamy shade to almost white (in a cardboard box 2, 3 or 6 blister packs of 10 tablets each, or 1, 2 or 4 blisters of 14 tablets each, or 1 polymer can or bottle 30, 60 or 100 tablets and instructions for the use of Rabeprazole-SZ).
Pellet composition (1 capsule of 10/20 mg, respectively):
- active substance: rabeprazole sodium - 10/20 mg (rabeprazole pellets - 118/236 mg, respectively);
- excipients: hydroxymethylcellulose - 14.75 / 29.5 mg; sodium carbonate - 1.65 / 3.3 mg; sugar crumbs (starch syrup, sucrose) - 71.47 / 142.94 mg; talc - 1.77 / 3.54 mg; titanium dioxide - 0.83 / 1.66 mg;
- shell: cetyl alcohol - 1.6 / 3.2 mg; hypromellose phthalate - 15.93 / 31.86 mg.
The composition of the capsule (10/20 mg, respectively):
- body: iron oxide yellow - 0 / 0.192%; titanium dioxide - 2/1%; gelatin - up to 100 / up to 100%;
- cap: dye azorubin - 0.661 9/0%; indigo carmine - 0.028 6/0%; titanium dioxide - 0.666 6 / 0.333 3%; iron oxide black - 0 / 0.53%; iron oxide yellow - 0 / 0.2%; iron oxide red - 0 / 0.93%; gelatin - up to 100 / up to 100%.
Pharmacological properties
Pharmacodynamics
Rabeprazole - the active substance of Rabeprazole-SZ, belongs to the benzimidazole derivatives, antisecretory substances. The main effects of the drug:
- suppression of gastric juice secretion: provided by specific inhibition of H + / K + -ATP-ase on the secretory surface of gastric parietal cells;
- blocking the final stage of hydrochloric acid secretion: the content of stimulated and basal secretion decreases, regardless of the etiology of the stimulus.
Due to its high lipophilicity, rabeprazole easily penetrates into the parietal cells of the stomach, where it is concentrated, as a result, the drug increases the secretion of bicarbonate and has a cytoprotective effect.
After oral administration of rabeprazole at a dose of 20 mg, the antisecretory effect develops within one hour, the maximum effect - in 2-4 hours. 23 hours after taking the first dose of Rabeprazole-SZ, inhibition of basal acid secretion is 62%, stimulated food - 82%. This effect lasts for about 48 hours. In case of termination of therapy, secretory activity is restored within 1-2 days.
The plasma concentration of gastrin in the blood increases during the first 2–8 weeks of treatment (which reflects the inhibitory effect on the secretion of hydrochloric acid). In 7-14 days after discontinuation of the drug, the value of this indicator returns to the initial level.
Rabeprazole has no anticholinergic properties; it does not affect the central nervous, respiratory and cardiovascular systems.
During therapy with rabeprazole, the development of stable changes in the severity of gastritis, in the morphological structure of enterochromaffin-like cells, in the frequency of atrophic gastritis, intestinal metaplasia, or the spread of Helicobacter pylori infection was not detected.
Pharmacokinetics
The substance is rapidly absorbed from the intestine, after ingestion of 20 mg of rabeprazole, C max (maximum concentration of the substance) in plasma is reached in approximately 3.5 hours. The change in plasma C max and AUC (area under the concentration-time curve) is linear when Rabeprazole-SZ is used in the dose range of 10–40 mg. The absolute bioavailability after oral administration of 20 mg of the substance (in comparison with intravenous administration) is approximately 52%. With repeated administration of rabeprazole, the value of this indicator does not change.
The time of day and simultaneous administration of antacids have no effect on the degree of absorption of rabeprazole. When the drug is taken with fatty foods, the absorption of rabeprazole slows down by 4 hours or more, but the values of C max and the degree of absorption remain unchanged.
The degree of binding of rabeprazole to plasma proteins in humans is approximately 97%.
T 1/2 (half-life) from plasma in healthy volunteers is in the range from 0.7 to 1.5 hours (an average of 1 hour), the total clearance is 3.8 ml / min / kg.
After a single oral dose of 20 mg of 14 C-labeled rabeprazole, no unchanged substance was found in the urine. Excretion of approximately 90% of rabeprazole occurs in the urine mainly in the form of two metabolites: carboxylic acid and mercapturic acid conjugate (M6 and M5, respectively). Also, two unknown metabolites are excreted, which were identified by toxicological analysis. The rest of the substance is excreted in the feces.
In total, 99.8% of rabeprazole is excreted. This indicates an insignificant excretion of metabolites with bile. The main metabolite (M1) is thioether. The only metabolite that is active is desmethyl (M3), but it was observed in only one study participant at a low concentration after taking 80 mg of rabeprazole.
With stable renal failure in the terminal stage in patients who need maintenance hemodialysis (with creatinine clearance <5 ml / min / 1.73 m 2), the excretion of the substance is similar to that in healthy volunteers. The C max and AUC values in these patients were approximately 35% lower than in healthy volunteers. Average T 1/2: healthy volunteers - 0.82 hours, patients during hemodialysis - 0.95 hours, patients after hemodialysis - 3.6 hours. The clearance of rabeprazole in patients with kidney disease who require hemodialysis is approximately 2 times higher than that in healthy volunteers.
The AUC value in patients with chronic liver damage is 2 times higher than in healthy volunteers, which indicates a decrease in the effect of the first passage through the liver, and T 1/2 from plasma is 2–3 times higher. Despite the fact that in patients with chronic compensated cirrhosis of the liver, the AUC is 2 times higher, and C max is 50% higher (in comparison with healthy volunteers), they tolerate the intake of 20 mg of rabeprazole once a day.
Elimination of the substance in elderly patients is somewhat slower. After 7 days of taking Rabeprazole-C3 in a daily dose of 20 mg, AUC in this group of patients increased approximately 2 times, C max - by 60%. At the same time, signs of rabeprazole cumulation are not observed.
Against the background of a slow metabolism of CYP2C19 after a week of using rabeprazole in a daily dose of 20 mg, AUC increases 1.9 times, and T 1/2 - 1.6 times in comparison with the same parameters in patients who are fast metabolizers, while while the value of C max increases by 40%.
Indications for use
- exacerbation of duodenal ulcer;
- exacerbation of gastric ulcer and anastomotic ulcer;
- erosive and ulcerative GERD (gastroesophageal reflux disease) in children from 12 years of age and adults or reflux esophagitis;
- GERD (supportive care);
- Zollinger-Ellison syndrome and other conditions characterized by pathological hypersecretion;
- NERD (non-erosive gastroesophageal reflux disease);
- eradication of Helicobacter pylori in patients with peptic ulcer disease (in combination with appropriate antibacterial drugs).
Contraindications
Absolute:
- deficiency of sucrase / isomaltase, fructose intolerance, glucose-galactose deficiency;
- pregnancy and the period of breastfeeding;
- age up to 12 (for the treatment of GERD) or 18 years (for other indications);
- individual intolerance to the components of the drug, as well as substituted benzimidazoles.
Relative (Rabeprazole-SZ capsules are prescribed under medical supervision):
- severe renal failure;
- severe liver failure.
Rabeprazole-SZ, instructions for use: method and dosage
Rabeprazole-SZ is taken orally, regardless of food intake and time of day. The capsules must be swallowed whole.
The dosage regimen is determined by the indications:
- exacerbation of duodenal ulcer: 20 mg once a day, for some patients to achieve a therapeutic effect, it is enough to take Rabeprazole-SZ at a dose of 10 mg. The therapy is carried out in a course of 2-4 weeks, according to indications, the drug intake can be extended for another 4 weeks;
- exacerbation of gastric ulcer and anastomotic ulcer: 10 or 20 mg 1 time per day. The cure usually occurs after 6 weeks of therapy, but sometimes the use of the drug continues for another 6 weeks;
- erosive and ulcerative GERD or reflux esophagitis: 10 or 20 mg once a day. Cure usually occurs after 4–8 weeks of therapy, but sometimes the drug is continued for another 8 weeks;
- GERD (maintenance treatment): 10 or 20 mg once a day. The duration of treatment is determined by the indications;
- NERD without esophagitis: 10 or 20 mg once a day. Usually the symptoms disappear after 4 weeks of therapy, if this does not happen, the patient is assigned an additional study. After relief of symptoms in order to prevent their subsequent development, Rabeprazole-SZ can be applied on demand 1 time per day, 10 mg;
- Zollinger-Ellison syndrome and other conditions characterized by pathological hypersecretion: the dose is selected individually. At the beginning of therapy, the use of Rabeprazole-SZ in a daily dose of 60 mg is indicated, then it is increased to 100 mg (in one dose) or 120 mg (in two equal doses); for some patients, fractional dosing is more preferred. The duration of therapy is determined by clinical necessity, in some cases it was carried out for 12 months;
- eradication of Helicobacter pylori in patients with peptic ulcer: 20 mg 2 times a day (Rabeprazole-SZ is used according to a specific scheme with an appropriate combination of antibiotics) for 7 days.
In patients with mild to moderate hepatic impairment, the concentration of rabeprazole in the blood is usually higher than in healthy volunteers. Care should be taken when prescribing Rabeprazole-SZ against the background of severe hepatic failure.
For children from 12 years of age in the treatment of GERD, the safety profile has been studied for a daily dose of 20 mg (at one time) for a course of up to 8 weeks.
Side effects
During clinical studies, the development of the following disorders was recorded: asthenia, dizziness, headache, rash, abdominal pain, flatulence, diarrhea, xerostomia.
Possible adverse reactions (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare; with an unknown frequency - to establish the frequency of violations seems possible):
- digestive system: often - constipation, flatulence, abdominal pain, vomiting, diarrhea, nausea; infrequently - belching, dyspepsia, xerostomia; rarely - taste disturbance, gastritis, stomatitis;
- hematopoietic system: rarely - neutropenia, thrombocytopenia, leukopenia;
- hepatobiliary system: rarely - jaundice, hepatitis, hepatic encephalopathy;
- immune system: rarely - acute systemic allergic reactions (including hypotension, facial edema, shortness of breath);
- nervous system: often - headache, insomnia, dizziness; infrequently - nervousness, drowsiness; rarely, depression; with an unknown frequency - confusion;
- respiratory system: often - pharyngitis, cough, rhinitis; infrequently - bronchitis, sinusitis;
- reproductive system: with an unknown frequency - gynecomastia;
- cardiovascular system: with an unknown frequency - peripheral edema;
- urinary system: infrequently - urinary tract infection; rarely - interstitial nephritis;
- skin and subcutaneous tissue: rarely - urticaria, bullous rash; very rarely - toxic epidermal necrolysis, erythema multiforme, Stevens-Johnson syndrome;
- musculoskeletal system: often - back pain; infrequently - arthralgia, myalgia, fracture of the bones of the thigh, spine or wrist, leg muscle cramps;
- organ of vision: rarely - visual impairment;
- metabolism: rarely - anorexia; with an unknown frequency - hypomagnesemia, hyponatremia;
- laboratory / instrumental studies: rarely - weight gain, increased activity of hepatic transaminases;
- others: often infections.
Overdose
Information on overdose is minimal.
Therapy: symptomatic and supportive. Rabeprazole is poorly excreted during dialysis, since it binds well to plasma proteins. The antidote is unknown.
special instructions
The patient's response to treatment with Rabeprazole-SZ does not exclude the presence of malignant neoplasms in the stomach.
When using the drug for at least 3 months, in rare cases, the development of asymptomatic or symptomatic hypomagnesemia was noted. Most often, these violations were reported one year after taking Rabeprazole-SZ. Serious adverse reactions included tetany, seizures, and arrhythmias. Most patients required hypomagnesemia therapy. It included replacement of magnesium and withdrawal of proton pump inhibitors, including Rabeprazole-SZ.
In patients undergoing long-term treatment or taking the drug in combination with digoxin or drugs that can lead to the development of hypomagnesemia (in particular, with diuretics), it is necessary to monitor the magnesium content before starting Rabeprazole-SZ and during the period of therapy.
During treatment, there may be an increased risk of fractures in the hip, spine, or wrist associated with osteoporosis. The risk is higher in patients who take high doses of Rabeprazole-SZ for a long time (12 months and longer).
According to the information in the literature, with the combined use of Rabeprazole-SZ with methotrexate (mainly in high doses), it is possible to increase the concentration of methotrexate and / or hydroxymethotrexate (its metabolite) and increase T 1/2, which can lead to the toxicity of methotrexate. If it is necessary to use high doses of methotrexate, the likelihood of temporary discontinuation of Rabeprazole-SZ should be considered.
Taking Rabeprazole-SZ may increase the risk of gastrointestinal infections, including infections caused by Salmonella, Clostridium difficile and Campylobacter.
Influence on the ability to drive vehicles and complex mechanisms
When driving vehicles and working with complex mechanisms, patients should take into account the likelihood of drowsiness.
Application during pregnancy and lactation
Rabeprazole-SZ capsules are not prescribed during pregnancy / lactation.
Pediatric use
Contraindication:
- up to 12 years: in the treatment of GERD;
- under 18 years of age: when used for other indications.
With impaired renal function
Rabeprazole-SZ is prescribed for patients with severe renal failure under medical supervision.
For violations of liver function
Rabeprazole-SZ is prescribed for patients with severe hepatic impairment under medical supervision.
Use in the elderly
Elderly patients do not need to adjust the dose.
Drug interactions
Possible interactions:
- phenytoin, diazepam, indirect anticoagulants (drugs metabolized by microsomal oxidation in the liver): slowing down their excretion;
- ketoconazole, itraconazole: the plasma concentration of these drugs can be significantly reduced;
- atazanavir: combination therapy is not recommended, since in this case the effect of atazanavir is significantly reduced;
- cyclosporine: rabeprazole inhibits its metabolism;
- methotrexate: an increase in the concentration of methotrexate and / or hydroxymethotrexate (its metabolite), as well as an increase in T 1/2;
- amoxicillin and clarithromycin: AUC and C max values for these drugs are similar when comparing monotherapy and combined use; AUC and C max of rabeprazole and the active metabolite of clarithromycin are increased (of no clinical significance).
Analogs
The analogues of Rabeprazole-SZ are: Ontime, Noflux, Bereta, Khairabezol, Rabelok, Pariet, Zulbeks, Rabiet, Zolispan, Razo, etc.
Terms and conditions of storage
Store in a place protected from light at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Rabeprazole-SZ
Reviews of Rabeprazole-SZ are mostly positive. It is noted that the drug has a long-term therapeutic effect and is well tolerated, causing side effects only in rare cases. Another advantage of the tool is considered a convenient dosing regimen. The cost in comparison with peers is estimated in different ways - from affordable to high.
Price for Rabeprazole-SZ in pharmacies
The approximate price for Rabeprazole-SZ for a package containing 14 capsules of 20 mg is 180 rubles.
Rabeprazole-SZ: prices in online pharmacies
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Drug name Price Pharmacy |
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Rabeprazole-SZ 10 mg enteric capsules 14 pcs. 92 RUB Buy |
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Rabeprazole-SZ 20 mg enteric capsules 14 pcs. 120 RUB Buy |
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Rabeprazole-SZ 10 mg enteric capsules 28 pcs. 183 r Buy |
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Rabeprazole-SZ enteric capsules. 20mg 14 pcs. 207 r Buy |
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Rabeprazole-SZ enteric capsules. 10mg 28 pcs. 210 RUB Buy |
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Rabeprazole-SZ 20 mg enteric capsules 28 pcs. RUB 298 Buy |
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Rabeprazole-SZ enteric capsules. 20mg 28 pcs. 334 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!
