Rabiet
Rabiet: 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: Rabiet
ATX code: A02BC04
Active ingredient: rabeprazole (Rabeprazole)
Producer: Obolensk JSC pharmaceutical company (Russia)
Description and photo update: 2018-27-11
Prices in pharmacies: from 194 rubles.
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Rabiet - an agent that suppresses the secretion of hydrochloric acid, an antiulcer drug.
Release form and composition
Dosage form - hard gelatin capsules: 10 mg dosage - size No. 3, with a blue cap and a white body; dosage 20 mg - size No. 1, with a blue cap and body. The contents of the capsules are spherical pellets from almost white to white with a yellowish or creamy shade. Capsules are packaged in 5, 7, 10, 14, 15, 20 and 30 pcs. in blisters, in a cardboard box 1, 2 or 3 packages and instructions for use Rabiet.
Composition of 1 capsule:
- active substance: rabeprazole sodium - 10 mg or 20 mg (in the form of pellets 8.5% - 118 mg or 236 mg);
- auxiliary components: sugar spheres (sucrose, povidone), talc, sodium carbonate, hypromellose, titanium dioxide;
- the composition of the pellet shell: cetyl alcohol, hypromellose phthalate;
- the composition of the capsule shell at a dosage of 10 mg: body - gelatin and titanium dioxide; cap - gelatin, titanium dioxide, patented diamond black and blue dyes;
- the composition of the capsule shell in a dosage of 20 mg: body and cap - gelatin, titanium dioxide, patented blue dye.
Pharmacological properties
Pharmacodynamics
The active component of Rabiet, sodium rabeprazole, belongs to the class of antisecretory compounds, is a benzimidazole derivative. Suppresses the secretion of gastric juice due to specific inhibition of H + / K + -ATPase (a protein complex that functions as a proton pump) on the secretory surface of gastric parietal cells. Thus, rabeprazole sodium inhibits the proton pump in the stomach and blocks the final stage of hydrochloric acid formation. The effectiveness of the drug is due to the dose and, regardless of the type of stimulus, its action leads to the suppression of both basal and stimulated acid secretion. Rabiet has no anticholinergic activity.
After taking Rabiet at a dose of 20 mg, the antisecretory effect develops within 1 hour. 23 hours after taking the first dose, the degree of inhibition of basal and stimulated acid secretion is 69% and 82%, respectively, the effect lasts up to 48 hours. The duration of the pharmacodynamic action of rabeprazole is much higher than predictable by the half-life (about 1 hour), which is explained by the prolonged binding of the drug with H + / K + -ATPase of parietal cells of the stomach. The value of the inhibitory effect of sodium rabeprazole on the secretion of hydrochloric acid reaches a plateau 3 days after the start of Rabiet administration. After its cancellation, the secretory activity is restored within 1–2 days.
The study on the effect of the drug on enterochromaffin-like cells involved 500 patients. They took rabeprazole sodium or a comparison drug for 8 weeks. According to the results, no stable changes were found in the frequency of atrophic gastritis and the severity of gastritis, in the spread of Helicobacter pylori infection, intestinal metaplasia and the morphological structure of enterochromaffin-like cells.
In a study on the effects of rabeprazole sodium on plasma gastrin levels, patients took Rabiet 10 mg and 20 mg daily for up to 43 months. In the first 2–8 weeks, the plasma concentration of gastrin was increased, which is explained by the inhibitory effect of the drug on acid secretion. Usually gastrin levels returned to baseline 1–2 weeks after stopping treatment.
In a study involving more than 400 patients who received rabeprazole sodium at a daily dose of 10 or 20 mg for 1 year, the incidence of hyperplasia was low and comparable to that with omeprazole (20 mg / kg). There were no cases of carcinoid tumors or adenomatous changes observed in rats.
Also, in the course of the studies, it was found that when taking Rabiet at 20 mg / day for 2 weeks, rabeprazole sodium does not affect carbohydrate metabolism, the level of parathyroid hormone in the blood, thyroid function, and the concentration of testosterone, estrogens, follicle-stimulating hormone, luteinizing hormone, prolactin, cortisol, glucagon, aldosterone, growth hormone and renin. There were no systemic effects of the drug on the central nervous, respiratory and cardiovascular systems.
Pharmacokinetics
Once in the intestines, rabeprazole is rapidly absorbed. The maximum plasma concentrations reach approximately 3.5 hours after taking a dose of 20 mg. Changes in maximum plasma concentrations (Cmax) and area under the concentration-time curve (AUC) are linear in the dose range of 10-40 mg.
After taking a dose of 20 mg, the absolute bioavailability is approximately 52%. With repeated administration of Rabiet, this indicator does not change.
The half-life of the drug from plasma in healthy volunteers is 0.7-1.5 hours (on average, 1 hour). The total clearance is 3.8 ml / min / kg.
In chronic liver damage, AUC is 2 times higher than in healthy volunteers, which indicates a decrease in metabolism during the first passage through the liver. In addition, the half-life in such patients is increased by 2–3 times.
The time of taking the drug and the simultaneous use of antacids does not affect the absorption of rabeprazole. Fatty foods taken with Rabiet delay the absorption of rabeprazole by at least 4 hours, but the degree of absorption and the maximum concentration do not change.
The connection with plasma proteins is about 97%.
After a single dose of 20 mg of 14C-labeled rabeprazole, unchanged drug was not detected in the urine of healthy volunteers. Approximately 90% of the substance is excreted by the kidneys, mainly in the form of two metabolites - the conjugate of mercapturic acid (M5) and carboxylic acid (M6), to a lesser extent - in the form of two unknown metabolites (they were found in toxicological analysis). The rest of the drug is excreted through the intestines. The total excretion is 99.8%, which indicates a small elimination of rabeprazole with bile. The main metabolite is thioether (M1). The only active metabolite is desmethyl (M3), but it was detected at a low concentration and in only one patient who took part in the study after taking a dose of Rabiet 80 mg.
Special patient groups:
- advanced age: the excretion of sodium rabeprazole is somewhat slowed down. After 7 days of taking the drug at a dose of 20 mg / day in elderly patients, the AUC was approximately 2 times more, Cmax was 60% higher compared with healthy younger volunteers. There were no signs of accumulation of the substance;
- CYP2C19 polymorphism: after 7 days of taking the drug at a dose of 20 mg / day in patients with slow metabolism, CYP2C19 AUC was increased by 1.9 times, the half-life was increased by 1.6 times compared with patients who are fast metabolizers. At the same time, Cmax increased by 40%;
- chronic compensated cirrhosis: AUC increases by 2 times, Cmax - by 50% compared with healthy volunteers. However, when taking the drug at a dose of 20 mg 1 time per day, rabeprazole was well tolerated;
- stable renal failure in the terminal stage in patients who require maintenance hemodialysis (creatinine clearance <5 ml / min / 1.73 m 2): AUC and Cmax are approximately 35% lower than in healthy volunteers. The elimination of rabeprazole is similar to that in healthy volunteers (during hemodialysis - 0.95 hours, after a session - 3.6 hours). The clearance of the drug is approximately 2 times higher than that of healthy volunteers.
Indications for use
Rabiet 10 mg capsules are used to treat the symptoms of dyspepsia associated with increased gastric acidity (including symptoms of gastroesophageal reflux disease), such as sour belching and heartburn.
Rabiet 20 mg capsules are prescribed in the following cases:
- peptic ulcer of the stomach and duodenum in the acute phase;
- anastomotic ulcer;
- reflux esophagitis;
- erosive and ulcerative gastroesophageal reflux disease (GERD);
- maintenance therapy for GERD;
- non-erosive GERD;
- Zollinger-Ellison syndrome and other conditions accompanied by pathological hypersecretion;
- eradication of Helicobacter pylori in peptic ulcer disease (in combination with antibiotic therapy).
Contraindications
- sucrose / isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption;
- age up to 12 years - for the treatment of GERD, up to 18 years - for other indications;
- the period of pregnancy and breastfeeding;
- hypersensitivity to drug components or substituted benzimidazoles.
With caution, Rabiet capsules should be used in severe renal failure.
Rabiet, application instruction: method and dosage
Rabiet capsules should be taken orally, swallowing whole (it is forbidden to grind or chew the capsules). Although the food intake and time of administration of the drug do not affect the activity of rabeprazole, it is recommended to take Rabiet in the morning before meals, which contributes to better patient compliance with the treatment regimen.
To treat the symptoms of dyspepsia associated with increased gastric acidity, 10 mg capsules are prescribed once a day. The duration of treatment without consulting a doctor should not exceed 14 days. If within 3 days the therapeutic effect of Rabiet is absent, you should consult a doctor.
Recommended dosage regimens of 20 mg capsules:
- anastomotic ulcer and exacerbation of gastric ulcer: 20 mg 1 time per day for 6 weeks, if necessary, the duration of therapy is increased to 12 weeks;
- exacerbation of duodenal ulcer: 20 mg 1 time per day for 2-4 weeks, if necessary, treatment is extended for another 4 weeks;
- reflux esophagitis and erosive GERD: 20 mg 1 time per day for 4-8 weeks, if necessary, therapy is extended for another 8 weeks;
- maintenance therapy for GERD: 20 mg once a day, the duration of treatment is determined individually depending on the patient's condition;
- non-erosive GERD without esophagitis: 20 mg 1 time per day, after relief of symptoms to prevent recurrence, Rabiet should be taken 1 time per day as needed. If symptoms persist after 4 weeks of taking the drug, the patient needs an additional examination;
- Zollinger-Ellison syndrome and other conditions with pathological hypersecretion: the dose is selected individually. Treatment usually begins with a daily dose of 60 mg, then it is increased to 100 mg 1 time per day or 60 mg 2 times a day if fractional dosing of the drug is more preferable. The duration of treatment can be up to 1 year;
- eradication of Helicobacter pylori: 20 mg 2 times a day in combination with antibiotics according to the scheme recommended by the doctor for 7 days.
Side effects
According to clinical studies, in general, Rabiet is well tolerated. The side effects that occur are usually mild to moderate and transient.
In clinical studies, the following adverse reactions have been reported:
- from the digestive system: dry mouth, flatulence, diarrhea or constipation, abdominal pain;
- from the nervous system: dizziness, headache;
- others: skin rashes, peripheral edema.
During the post-registration period, the following side effects were also identified:
- from the digestive system: increased activity of liver enzymes; rarely - jaundice, hepatitis; in patients with liver cirrhosis - hepatic encephalopathy;
- from the musculoskeletal system: rarely - arthralgia, myalgia;
- from the hematopoietic system: rarely - neutropenia, thrombocytopenia, leukopenia;
- allergic reactions: rarely - urticaria, bullous rashes, acute systemic allergic reactions; very rarely - Stevens-Johnson syndrome, toxic epidermal necrolysis, erythema multiforme;
- others: rarely - hypomagnesemia; very rarely - gynecomastia, interstitial nephritis, increased risk of fractures.
Overdose
Cases of severe overdose are unknown.
When taking a dose that is significantly higher than the recommended one, symptomatic and supportive therapy is indicated. The specific antidote has not been established. Dialysis is ineffective because rabeprazole binds well to blood plasma proteins.
special instructions
In patients receiving proton pump inhibitors (PPIs) for 3 months or more, in rare cases, symptomatic and asymptomatic hypomagnesemia is detected. Most of the reports were received one year after treatment. Arrhythmia, tetany, and seizures have been reported as serious side effects. Most of the patients required discontinuation of PPIs and the appointment of treatment, including magnesium replacement. In this regard, with prolonged use of Rabiet or the simultaneous use of drugs that can cause hypomagnesemia (for example, diuretics or digoxin), patients need to control the concentration of magnesium in the blood.
During the period of therapy, you should not take other PPIs and drugs that reduce gastric acidity, for example, H 2 -histamine receptor blockers.
Improving the patient's condition while taking Rabiet does not exclude the presence of malignant neoplasms in his stomach.
According to post-marketing surveillance data, PPI use may increase the risk of wrist, spine, or hip fractures associated with osteoporosis. The risk increases with the use of PPIs in high doses (exceeding those recommended in the instructions) for a long time (from 1 year).
Reception of Rabiet is a risk factor for the development of gastrointestinal infections, such as Clostridium difficile.
Patients who have recurring symptoms of heartburn or digestive problems are advised to see a doctor regularly.
If you need to take other over-the-counter medicines while using Rabiet, you should consult a pharmacist or healthcare professional.
Patients should refrain from taking Rabiet before the urea breath test.
Patients requiring an endoscopic examination should inform their doctor if they are taking rabeprazole.
When Rabiet is taken without a prescription for short-term symptomatic treatment of manifestations of non-erosive reflux disease or gastroesophageal reflux disease (such as heartburn), it is recommended that you consult your doctor if:
- long-term treatment - for 4 or more weeks;
- the appearance of new symptoms or a change in previously observed symptoms in patients over the age of 55;
- weight loss, anemia, pain when swallowing, dysphagia, bleeding in the gastrointestinal tract, constant vomiting or vomiting with epigastric and blood contents;
- a history of liver / kidney dysfunction, jaundice, stomach ulcers, or stomach surgery.
People over the age of 55 who take daily over-the-counter medications to relieve symptoms of indigestion and heartburn should inform their healthcare professional.
Influence on the ability to drive vehicles and complex mechanisms
Given the pharmacodynamic parameters of rabeprazole and the profile of its undesirable effects, it is unlikely that Rabiet will affect the speed of reactions and the ability to concentrate. Patients who experience drowsiness during the treatment period are advised to refrain from driving a car and performing potentially dangerous types of work.
Application during pregnancy and lactation
In reproductive studies, signs of impaired fertility and fetal defects in rabbits and rats were not detected. However, in rats, the drug penetrated the placental barrier. There is no data to support the safety of rabeprazole in pregnant women. For this reason, during pregnancy, the use of Rabiet is contraindicated, except in cases where the expected benefit from therapy for the woman is definitely higher than the potential risks to the fetus.
Whether rabeprazole is excreted in a woman's breast milk has not been established, since relevant studies have not been conducted. Rabeprazole was found in the milk of lactating rats, therefore Rabiet is contraindicated for use during lactation.
Pediatric use
Rabiet 10 mg capsules, used to treat symptoms of dyspepsia associated with increased gastric acidity, are not prescribed for children and adolescents under the age of 18.
The efficacy and safety of 20 mg capsules in children over 12 years of age when used for the treatment of GERD has been confirmed by adequate and well-controlled studies for short-term treatment (up to 8 weeks). The safety and effectiveness of rabeprazole in pediatrics for other indications has not been established.
With impaired renal function
In severe renal failure, Rabiet should be used with caution. No dose adjustment is required.
For violations of liver function
In mild and moderate liver dysfunctions, there were no significant differences in the incidence of side effects from that in healthy patients of the same sex and age.
At the first appointment of Rabiet to persons with severely impaired liver function, it is recommended to be careful. No dose adjustment is required, but it should be borne in mind that the AUC of rabeprazole sodium is approximately 2 times higher than that of healthy volunteers.
Patients with severe hepatic impairment are advised to consult a doctor before using Rabiet for short-term symptomatic therapy on their own.
Use in the elderly
No dose adjustment of Rabiet is required for elderly patients.
Drug interactions
According to the literature, in the case of taking rabeprazole simultaneously with methotrexate (mainly in high doses), it is possible to increase the concentration of methotrexate and / or its main metabolite, hydroxymethotrexate, and increase the time of its excretion. In this regard, if it is necessary to use high doses of methotrexate, the option of temporarily canceling Rabiet should be considered.
In the study of combination therapy with antibiotics (amoxicillin, clarithromycin), some changes in the maximum concentrations of drugs and the area under the concentration-time curve were revealed, but they were not recognized as clinically significant.
In vitro studies have shown that rabeprazole inhibits the metabolism of cyclosporine with an IC 50 of 62 μmol, i.e., at a concentration that is 50 times higher than the maximum concentration in healthy volunteers after 20 days of taking rabeprazole at a daily dose of 20 mg. The degree of inhibition is similar to that of omeprazole at similar concentrations.
Rabeprazole sodium causes a sustained and long-term suppression of gastric acid secretion, therefore it can interact with drugs, the absorption of which depends on the pH level. The absorption of atazanavir is also pH dependent. Although its concomitant use with rabeprazole has not been studied, a significant decrease in its effect is expected. For this reason, concomitant administration of drugs is not recommended.
Rabeprazole sodium is metabolized in the liver with the participation of the cytochrome P450 system (CYP450). However, in vitro the drug did not have clinically significant interactions with other drugs that are also metabolized by this system, such as warfarin, phenytoin, diazepam, theophylline.
No clinically significant interactions of rabeprazole with antacids have been observed.
Analogs
The analogues of Rabiet are Bereta, Zulbeks, Noflux, Pariet, Rabelok, Rabeprazole-OBL, Rabeprazole-C3, Razo, Khairabezol, Nexium, Esomeprazole, Emesol, Sanpraz, Pantaz, Peptazol, Ultop, Promez, Omefazol, Omezoprazol, Limeprazol, Lancid, Epicurus, etc.
Terms and conditions of storage
Store at temperatures up to 25 ° C in a dry place, protected from light and out of reach of children.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Available without a prescription.
Reviews about Rabiet
Reviews about Rabiet are mostly positive. Patients note that the drug effectively eliminates the symptoms caused by increased gastric acidity, has a long-term effect, and is inexpensive.
Price for Rabiet in pharmacies
Approximate prices of Rabiet: 10 mg capsules (14 pieces per package) - 119-180 rubles, 20 mg capsules (14 pieces per package) - 208-309 rubles.
Rabiet: prices in online pharmacies
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Drug name Price Pharmacy |
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Rabiet 10 mg enteric capsules 14 pcs. 194 r Buy |
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Rabiet 20 mg enteric capsules 14 pcs. 299 r Buy |
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Rabiet capsules of intestinal products. 10mg 14 pcs. 302 RUB Buy |
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Rabiet capsules of intestinal products. 20mg 14 pcs. 419 RUB Buy |
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Rabiet 20 mg enteric capsules 28 pcs. 502 RUB Buy |
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Rabiet capsules of intestinal products. 20mg 28 pcs. 582 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
