Pariet
Pariet: 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: Pariet
ATX code: A02BC04
Active ingredient: rabeprazole (rabeprazole)
Manufacturer: Bushu Pharmaceuticals Ltd. (Bushu Pharmaceuticals Ltd.) (Japan), Eisai Co. Ltd. (Eisai Co. Ltd.) (Japan)
Description and photo update: 02.10.2019
Prices in pharmacies: from 541 rubles.
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Pariet is a proton pump inhibitor (PPI), a drug that reduces gastric secretion.
Release form and composition
Dosage form Pariet - enteric-coated tablets: rounded, convex on both sides:
- 10 mg - pink with a black “E241” mark on one side; on a cross section, a tablet is almost white or white (7 or 14 pcs. in blisters, 1 or 2 blisters are placed in a cardboard box);
- 20 mg - light yellow, marked with red “E243” on one side; on a cross-section, a tablet is almost white or white (7 or 14 pieces in blisters, 1 or 2 blisters are placed in a cardboard box).
Active ingredient: sodium rabeprazole, its content in 1 tablet is 10 mg (which corresponds to 9.42 mg of rabeprazole) or 20 mg (which corresponds to 18.85 mg of rabeprazole).
Additional substances: magnesium oxide, diacetylated monoglyceride, titanium dioxide (E171), talc, hydroxypropyl cellulose (hyprolose), magnesium stearate, weakly substituted hydroxypropyl cellulose (hyprolose), mannitol (mannitol), hypromellose phthalate, ethylcellulose red, iron dye carna tablets 10 mg) or iron oxide yellow (in tablets 20 mg), food gray ink F6 (in tablets 10 mg - iron oxide black, shellac white, dehydrated ethanol, 1-butanol) or red food ink A1 (in tablets 20 mg - iron oxide red, shellac white, ester of glyceric acid, carnauba wax, dehydrated ethanol, 1-butanol).
Pharmacological properties
Pariet is one of the drugs that lower the secretion of gastric glands. It is a proton pump inhibitor.
Pharmacodynamics
Rabeprazole sodium belongs to the class of antisecretory substances derived from benzimidazole. Suppresses the secretion of gastric juice, which occurs due to the specific inhibition of H + / K + -ATPase (adenosine triphosphatase) on the secretory surface of the parietal cells of the stomach. The H + / K + -ATPase is a protein complex that functions like a proton pump. Rabeprazole sodium thus inhibits the proton pump in the stomach and blocks the final stage of acid production. This action is dose-dependent. Basal and stimulated acid secretion is suppressed regardless of the stimulus. The substance does not possess anticholinergic properties.
The antisecretory effect after oral administration of 20 mg of rabeprazole sodium develops within 60 minutes. Inhibition of acid secretion (basal and stimulated) 23 hours after taking the first dose of Pariet is 69 and 82%, respectively. Duration of action - up to 48 hours. This duration of the therapeutic effect is slightly higher than predicted by T 1/2 (half-life). This can be explained by the prolonged binding of rabeprazole sodium to the H + / K + -ATPase of gastric parietal cells. The magnitude of the inhibitory effect of rabeprazole sodium on acid secretion reaches a constant plasma concentration as a result of three days of therapy. After the end of the reception of Pariet, the secretory activity is restored in 1-2 days.
When conducting clinical studies, the effect of therapy (daily intake of 10 or 20 mg of rabeprazole sodium for a course of up to 43 months) on the level of gastrin in plasma was studied. According to the results, an increase in the plasma gastrin level was noted in the first 2–8 weeks of use, which is an indicator of an inhibitory effect on acid secretion. 1-2 weeks after stopping treatment, the concentration of gastrin usually returns to its original value.
When conducting studies on the effect on enterochromaffin-like cells, it was found that after 8 weeks of therapy, no stable changes in the frequency of atrophic gastritis, the morphological structure of enterochromaffin-like cells, the severity of gastritis, the spread of Helicobacter pylori infection or intestinal metaplasia were found.
After treatment for one year at therapeutic doses, the incidence of hyperplasia remained low and comparable to that of omeprazole (for a dose of 20 mg / kg).
Any systemic disorders in relation to the nervous, respiratory or cardiovascular systems associated with the intake of rabeprazole sodium have not yet been identified.
It has been proven that therapy with rabeprazole sodium for two weeks at a daily dose of 20 mg does not affect the following indicators: the level of parathyroid hormone in the blood, carbohydrate metabolism, thyroid function, as well as the level of most hormones, including glucagon, cortisol, estrogens, prolactin, testosterone, renin, aldosterone, follicle-stimulating, luteinizing and growth hormone.
Pharmacokinetics
After oral administration, rabeprazole is rapidly absorbed from the intestine, its C max (maximum plasma concentration) is reached approximately 3.5 hours after taking a dose of 20 mg. The change in C max and AUC (area under the concentration-time curve) in the dose range of 10–40 mg is linear. The absolute bioavailability after oral administration of 20 mg rabeprazole (compared to intravenous administration) is approximately 52%. With repeated administration of the drug, bioavailability does not change. The T 1/2 (half-life) from plasma in healthy volunteers is approximately 1 hour (in the range of 0.7-1.5 hours); total clearance - 3.8 ml / min / kg.
In case of chronic liver damage, AUC in comparison with the value of the indicator in healthy volunteers increases by 2 times. This is evidence of a decrease in first pass metabolism. In this case, T 1/2 from plasma increases by a factor of 2–3. The time of taking the drug or combined therapy with antacids does not affect the absorption of rabeprazole. Fatty foods slow down the absorption of rabeprazole by 4 hours or longer, but the C max values and the degree of absorption do not change.
The degree of binding of rabeprazole to plasma proteins is approximately 97%.
Approximately 90% of rabeprazole in healthy people is excreted in the urine mainly in the form of two metabolites: a conjugate of mercapturic acid (M5) and carboxylic acid (M6). Also, during the toxicological analysis, two unknown metabolites were identified. The remainder of the dose is excreted in the feces. In total, 99.8% of the substance is excreted in the urine and feces, which indicates a small excretion of metabolites of the substance with bile, the main of which is thioester (M1). Rabeprazole has a single active metabolite, desmethyl (M3), but it was found in low concentration in only one study participant after taking a dose of 80 mg.
When stable renal disease in the terminal stage, if necessary maintenance hemodialysis (when creatinine clearance <5 ml / min / 1,73m 2) excretion of sodium rabeprazole has no differences from values typical for healthy volunteers. The AUC and C max levels in this group of patients are approximately 35% lower than in healthy volunteers. The average T 1/2 of rabeprazole is: in healthy volunteers - 0.82 hours; in patients during hemodialysis - 0.95 hours; after hemodialysis - 3.6 hours. The clearance of rabeprazole sodium in patients requiring hemodialysis with kidney disease is approximately 2 times higher than in healthy volunteers.
In chronic compensated liver cirrhosis, rabeprazole sodium 1 time per day at a dose of 20 mg is well tolerated, although the AUC value is doubled and C max is increased by 50% in comparison with healthy volunteers.
Elderly patients have a slightly slower elimination of rabeprazole. After 7 days of therapy in a daily dose of 20 mg, AUC increases by about 2 times, and C max - by 60% in comparison with healthy young volunteers. At the same time, signs of rabeprazole cumulation are not observed.
Against the background of a slowed metabolism of CYP2C19 after 7 days of therapy in a daily dose of 20 mg, AUC increases 1.9 times, T 1/2 - 1.6 times, at the same time the C max value increases by 40%.
Indications for use
Pariet tablets in a dosage of 10 mg are recommended for the symptomatic treatment of dyspepsia caused by increased acidity of gastric juice, including for the treatment of symptoms of gastroesophageal reflux disease (GERD) such as heartburn and sour belching.
Indications for the use of Pariet tablets at a dosage of 20 mg:
- Anastomotic ulcer;
- Exacerbation of gastric ulcer and 12 duodenal ulcer;
- Reflux esophagitis, erosive and ulcerative gastroesophageal reflux disease;
- Non-erosive gastroesophageal reflux disease (NERD);
- Zollinger-Ellison syndrome and other conditions with pathological hypersecretion;
- Supportive therapy for gastroesophageal reflux disease;
- Eradication of Helicobacter pylori in patients with peptic ulcer disease.
Contraindications
Absolute:
- the period of pregnancy and lactation (breastfeeding);
- children's age: 10 mg tablets - up to 18 years, 20 mg tablets - up to 12 years;
- increased individual sensitivity to substituted benzimidazoles, rabeprazole, excipients of the drug.
A relative contraindication for the use of Pariet is severe renal failure; also, with caution, 20 mg tablets should be prescribed in children and adolescents from 12 to 18 years.
Instructions for the use of Pariet: method and dosage
Pariet is intended for oral administration. The tablets should be swallowed whole, without crushing or chewing, and washed down with water, preferably in the morning before eating. It was found that the time of day and food intake did not affect the activity of rabeprazole, but the recommended time of taking the drug promotes patient compliance with treatment regimens.
Tablets in a dosage of 10 mg are recommended for the symptomatic treatment of dyspepsia caused by increased acidity of gastric juice, including symptoms of GERD, 10 mg 1 time per day for a course of up to 14 days. If there is no clinically significant effect during the first 3 days of taking Pariet, you should consult a specialist.
Standard dosage regimens for 20 mg tablets for the treatment of adult patients, depending on the indication:
- Anastomotic ulcer, exacerbation of peptic ulcer: 20 mg 1 time per day. The duration of treatment is 6 weeks, if necessary, the course can be extended for another 6 weeks;
- Exacerbation of duodenal ulcer: 20 mg 1 time per day. The duration of treatment is 2-4 weeks, if necessary, the course is extended for another 4 weeks;
- Reflux esophagitis, erosive GERD: 20 mg 1 time per day for 4-8 weeks, if necessary, the duration of treatment is increased by another 8 weeks;
- Maintenance therapy for GERD: 20 mg 1 time per day, the duration of use is determined individually;
- Non-erosive reflux disease without esophagitis: 20 mg 1 time per day for 4 weeks. If after this time the symptoms of the disease do not disappear, it is necessary to conduct an additional examination of the patient. With maintenance therapy (after relief of symptoms to prevent relapse), take 1 tablet 1 time per day on demand;
- Zollinger-Ellison syndrome and other conditions characterized by pathological hypersecretion: the dose is selected individually. At the beginning of therapy, 60 mg per day is prescribed, then the dose is increased to 100 mg 1 time per day or 60 mg 2 times a day. The duration of treatment is determined by clinical necessity, in some cases it can reach 1 year;
- Eradication of Helicobacter pylori: 20 mg 2 times a day in combination with antibiotics. The course of treatment is 7 days.
Children over the age of 12 with GERD are prescribed 1 Pariet tablet at a dosage of 20 mg 1 time per day for a course of no more than 8 weeks.
Side effects
According to clinical studies, Pariet is generally well tolerated. Side effects are rare, usually mild to moderate, and transient.
In rare cases, the following adverse reactions occur:
- From the immune system: acute systemic allergic reactions;
- From the blood and lymphatic system: neutropenia, thrombocytopenia, leukopenia;
- From the side of metabolism and nutrition: hypomagnesemia;
- From the digestive system: diarrhea / constipation, flatulence, abdominal pain, dry mouth;
- From the central nervous system: headache;
- From the hepatobiliary system: increased activity of hepatic enzymes, jaundice, hepatitis, hepatic encephalopathy;
- From the kidneys and urinary tract: interstitial nephritis;
- Skin and subcutaneous tissue disorders: urticaria, bullous rash, erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis;
- From the musculoskeletal system: myalgia, arthralgia;
- From the reproductive system: gynecomastia.
Overdose
Information about accidental or intentional overdose is minimal. Cases of severe overdose with rabeprazole are unknown.
Therapy: symptomatic and supportive. There is no specific antidote. It must be borne in mind that rabeprazole has a high bond with plasma proteins, therefore, it is poorly excreted during dialysis.
special instructions
The patient's response to therapy with Pariet does not exclude the presence of malignant neoplasms in the stomach.
In patients who take Pariet or will receive it for a long time simultaneously with digoxin or drugs that can cause hypomagnesemia (for example, diuretics), the level of magnesium in the blood should be monitored before prescribing a proton pump inhibitor and for the entire period of its use.
Do not take simultaneously other drugs that reduce acidity, including blockers of H 2 -receptors.
Observational studies suggest that PPIs increase the risk of osteoporosis-related fractures of the wrist, hip and spine. This risk is especially high in patients who receive high-dose PPIs for a long period (1 year or more).
PPI use can increase the risk of developing gastrointestinal infections such as Clostridium difficile.
Patients who take Pariet without a doctor's prescription for short-term symptomatic treatment of symptoms of GERD and NERD (eg, heartburn) should consult a doctor in the following cases:
- Changes in previously observed signs of the disease or the appearance of new symptoms in patients over the age of 55;
- Long-term use of the drug (for 4 weeks or more) to relieve symptoms of indigestion and heartburn;
- The occurrence of anemia, pain when swallowing, bleeding in the gastrointestinal tract, persistent vomiting or vomiting with epigastric contents and blood, dysphagia;
- Cases of unintentional weight loss, jaundice, as well as a history of stomach ulcers or stomach surgery, etc.
Patients with severely impaired liver function should consult a doctor before using Pariet for short-term symptomatic treatment of manifestations of GERD and NERD (eg, heartburn).
Patients who suffer from recurring symptoms of heartburn or indigestion for a long time should be monitored regularly by a doctor.
People over the age of 55 should tell their healthcare provider if they are taking daily over-the-counter drugs (including Pariet) to reduce heartburn and symptoms of indigestion.
Patients who are receiving any other medications should consult with their doctor or pharmacist before taking Pariet.
Patients who are scheduled for endoscopy should warn their doctor if they are taking Pariet without a prescription.
Pariet should not be used before the urea breath test.
Influence on the ability to drive vehicles and complex mechanisms
Given the pharmacodynamics of rabeprazole and its side effect profile, it is unlikely that Pariet has a negative effect on reaction rate and ability to concentrate.
Application during pregnancy and lactation
According to the instructions, Pariet is not prescribed during pregnancy / lactation.
In exceptional cases, if the expected benefit to the expectant mother is estimated to be higher than the potential harm to the fetus, it is possible to use Parieta during pregnancy.
Pediatric use
Tablets at a dosage of 10 mg are contraindicated in pediatrics for the treatment of children and adolescents under 18 years of age.
Safety and efficacy of 20 mg tablets:
- treatment of GERD in children 12 years and older (provided that it is taken once a day for a short course of no more than 8 weeks) - confirmed by extrapolation of the results of well-controlled adequate studies of treatment of adult patients, as well as by studying the safety of use and pharmacokinetic characteristics in pediatric practice;
- treatment of GERD in children under 12 years of age - not established;
- use in pediatrics for other indications (for patients under 18 years of age) - not established.
With impaired renal function
Patients with impaired renal function do not require dose adjustment.
For patients with severe renal failure, Pariet in a dosage of 10 mg is prescribed with caution.
For violations of liver function
With mild to moderate liver failure, there is an increased level of rabeprazole in the blood compared to that in healthy patients. Appointment of the drug Pariet in severe liver failure requires caution.
Use in the elderly
Elderly patients do not require dose adjustment of Parieta.
Drug interactions
With simultaneous use, rabeprazole can increase the concentration of methotrexate and / or hydroxymethotrexate (its metabolite) and increase their half-life, as a result of which the toxicity of methotrexate may increase. If it is necessary to prescribe the latter in high doses, it is necessary to consider the possibility of temporary cancellation of PPIs.
Rabeprazole inhibits the metabolism of cyclosporine.
With the simultaneous use of atazanavir or ritonavir simultaneously with omeprazole or lansoprazole, a significant decrease in the effect of atazanavir was noted. Although reactions with rabeprazole have not been studied, similar results are expected.
Rabeprazole inhibits gastric acid secretion, therefore it can interact with substances, the absorption of which depends on pH. For example, with the simultaneous use of rabeprazole, it reduces the absorption of ketoconazole by 30%, and increases the absorption of digoxin by 22%. For this reason, if it is necessary to use such combinations, treatment should be carried out under close supervision and, if the need arises, the doses of drugs should be adjusted.
Food enriched with fats can slow down the absorption of rabeprazole for up to 4 hours or more, but the maximum and total concentration of the substance in the blood plasma does not change.
Analogs
Pariet analogs are: Bereta, Rabeprazole, Razo, Omeprazole, Ranitidine, Famotidine, Nexium, Noflux, Khairabezol.
Terms and conditions of storage
Store at temperatures up to 25 ºС out of reach of children. Do not freeze.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Available without a prescription.
Reviews about Pariet
Most of the reviews about Pariet are positive. Its high efficiency and good tolerance are noted. The main disadvantage in most cases is the high cost. The development of side effects is reported only in isolated cases.
Price for Pariet in pharmacies
The approximate price for Pariet is:
- tablets 10 mg: 7 pcs. - 788-1170 rubles; 14 pcs. - 1288-1322 rubles;
- tablets 20 mg: 7 pcs. - 836 rubles, 14 pcs. - 1954-2002 rubles.
Pariet: prices in online pharmacies
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Drug name Price Pharmacy |
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Pariet 10 mg enteric-coated tablets 7 pcs. 541 r Buy |
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Pariet 10 mg enteric coated tablets 14 pcs. 1368 RUB Buy |
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Pariet tablets p.p. 10mg 14 pcs. 1560 RUB Buy |
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Pariet 20 mg enteric coated tablets 14 pcs. 2052 RUB Buy |
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Pariet tablets p.p. 20mg 14 pcs. 2301 RUB Buy |
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Pariet 20 mg enteric-coated tablets 28 pcs. 3809 RUB Buy |
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Pariet tablets p.p. 20mg 28 pcs. 4073 RUB 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!
