Pariet 20mg 14 enteric tablets— Made in Switzerland — Free Delivery

(Pariet )
Pariet 20mg 14 enteric tablets— Made in Switzerland — Free Delivery
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Janssen-Silag Brand: Janssen-Silag
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Description Pariet 20mg 14 enteric tablets— Made in Switzerland — Free Delivery

Pharmacological properties

Pariet belongs to the class of antisecretory compounds, which are chemically substituted benzimidazoles, suppresses gastric acid secretion by specifically inhibiting the h + / k + -atphase enzyme on the secretory surface of gastric parietal cells. this enzyme system is considered an acid (proton) pump, therefore pariet is classified as an inhibitor of the gastric proton pump, which blocks the final stage of gastric acid production. the preparation does not have anticholinergic activity and is not an antagonist of histamine H2-receptors. it was experimentally established that after the introduction of rabeprazole sodium into the body quickly disappears both from the blood plasma and from the gastric mucosa. rabeprazole sodium has a slightly alkaline reaction, is rapidly absorbed in the digestive tract and is concentrated in parient cells. rabeprazole sodium is converted to the active sulfenamide form by protonation and thus reacts with the available cysteine ​​residues of the proton pump.

Antisecretory activity

After oral administration of 20 mg of Pariet, the antisecretory effect occurs within 1 hour and reaches a maximum after 2–4 hours. Inhibition of basal and food-stimulated secretion of gastric acid 23 hours after taking the first dose of Pariet was 62 and 82%, respectively, and the duration of this effect reached 48 hours. The inhibitory effect of Pariet on the secretion of gastric acid increases slightly during the daily intake of 1 tablet, and a stable inhibition of secretion is achieved 3 days after the start of taking this preparation. After the end of the reception of Pariet, secretory activity is normalized within 2-3 days.
Effect on serum gastrin concentration
In clinical trials, patients took 10 or 20 mg of Pariet 1 time per day for up to 12 months. During the first 2–8 weeks of therapy, the serum gastrin concentration increased, reflecting the inhibition of gastric acid secretion. The concentration of gastrin was restored to the initial level, usually within 1–2 weeks after the end of treatment. The study of biopsies of the fundus and antrum of the stomach in more than 500 patients who received Pariet or the reference preparation for up to 8 weeks did not reveal any histological changes, the severity of gastritis, the frequency of atrophic gastritis, intestinal metaplasia, and the prevalence of H. pylori infection. With long-term treatment for 36 months, more than 250 patients also showed no significant changes in the results of these studies.

Absorption

Due to the special dosage form, the absorption of sodium rabeprazole occurs in the intestine. This dosage form protects rabeprazole sodium from the effects of hydrochloric acid, which breaks down this compound. It is rapidly absorbed from the intestine and its peak plasma concentrations are reached approximately 3.5 hours after ingestion of a 20 mg dose. The maximum plasma concentration and AUC of rabeprazole are linear in the dose range of 10–40 mg. The absolute bioavailability after oral administration of 20 mg (compared to intravenous administration) is about 52%, largely due to first pass metabolism through the liver. In addition, bioavailability does not increase with repeated administration of Pariet. In healthy volunteers, the plasma elimination half-life was approximately 1 hour (from 0.7 to 1.5 hours), and the total clearance was 283 ± 98 ml / min. Absorption of Parieta does not depend on food intake and time of administration of the preparation. The degree of binding of rabeprazole sodium to blood plasma proteins reaches 97%. The main metabolites detected in blood plasma are thioester and carboxylic acid, while secondary metabolites, which are detected at low concentrations, are sulfone, dimethylthioethyl, and mercapturic acid conjugate. Only the dimethyl metabolite (M3) has an insignificant antisecretory activity, but it is not detected in the blood plasma. After a single dose of 20 mg, rabeprazole is not detected in the urine in an unchanged form. Approximately 90% of the administered dose is eliminated in the urine mainly in the form of two metabolites: a conjugate of mercapturic acid and carboxylic acid; in addition, experimental studies have identified two more unidentified metabolites. The rest of the preparation  is excreted in the feces. The pharmacokinetics of rabeprazole in men and women are not different.

Renal failure

In patients with stable end-stage renal disease requiring maintenance hemodialysis, the distribution of the Pariet was very similar to that in healthy volunteers. The AUC of rabeprazole sodium and the maximum blood concentration for these patients were almost 35% increased compared with those in healthy volunteers. The half-life averaged 0.82 h in healthy volunteers, 0.95 h in hemodialysis patients, and 3.6 h after dialysis. The dose calculated for patients with renal failure on hemodialysis was approximately twice that of healthy volunteers.

Liver failure

After a single dose of Pariet 20 mg in patients with moderate chronic liver damage compared with healthy volunteers, the AUC doubled and there was a 2-3-fold increase in the half-life of rabeprazole sodium. Thus, with a daily intake of the preparation at a dose of 20 mg for 7 days, the AUC should increase by at least 1.5 times and the maximum plasma concentration should increase to 1.2. The half-life of Pariet in patients with liver damage was 12.3 hours compared to 2.1 hours in healthy volunteers. The pharmacodynamic response (pH-metry of gastric juice) for individuals of both groups was therapeutically comparable.
In elderly patients, elimination of the preparation  is somewhat slower. After 7 days of taking rabeprazole sodium at a dose of 20 mg / day in the elderly, the AUC was approximately twice as high, and the maximum plasma concentration increased by 60% compared to that in healthy young volunteers. However, there are no signs of accumulation of rabeprazole sodium.
Currently, there is no data on the development of systemic effects from the central nervous system, cardiovascular and respiratory systems caused by the use of sodium rabeprazole. Oral administration of rabeprazole sodium at a dose of 20 mg / day for 2 weeks did not affect the function of the thyroid gland, carbohydrate metabolism, as well as the concentration in the blood of parathyroid hormone, cortisone, estrogen, testosterone, prolactin, cholecystokinin, secretin, glucagon, FSH, LH, renin, aldosterone and growth hormone.
CYP2C19 polymorphism
When rabeprazole sodium was prescribed at a dose of 20 mg / day for 7 days in patients with reduced CYP2C19 activity, the AUC value and elimination half-life were approximately 1.9 and 1.6 times higher, respectively, compared with patients with a rapid metabolism of rabeprazole; at the same time, the maximum plasma concentration increased by only 40%.

Indications

Peptic ulcer localized in the stomach or duodenum; gastroesophageal reflux disease (peptic ulcer of the esophagus, erosive esophagitis); in combination with antibacterial agents for the eradication of h.pylori in patients with peptic ulcers and chronic gastritis, for the healing of an ulcer and for the prevention of recurrence of peptic ulcers associated with h.pylori.

Application

Adults, including elderly patients, with active peptic ulcers of the stomach and duodenum are prescribed 1 tablet (20 mg) 1 time per day in the morning. the duration of taking the preparation for peptic ulcer of the duodenum is on average 4 weeks (in the absence of scarring - up to 8 weeks).
Most patients with peptic gastric ulcers heal within 6 weeks, but some patients may require additional Pariet for another 6 weeks.
For gastroesophageal reflux disease or gastroesophageal ulcerative reflux disease, 1 tablet of Pariet (20 mg) is prescribed 1 time per day for 4–8 weeks. The maintenance dose for this pathology is 20 mg / day for a long time.
The following treatment regimens are recommended for H. pylori eradication:
Pariet 20 mg 2 times a day + clarithromycin 500 mg 2 times a day + amoxicillin 1 g 2 times a day for 7 days;
Pariet 20 mg 2 times a day + clarithromycin 500 mg 2 times a day + metronidazole 400 mg 2 times a day for 7 days.
The optimal eradication result (in more than 90% of cases) was observed when using the first scheme.
Eradication of H. pylori by any of the above schemes leads to scarring of peptic duodenal ulcers or gastric ulcers without the need for additional continuation of antiulcer therapy.
The tablets are taken in the morning, before meals, without chewing or crushing.
Moderately severe liver or kidney dysfunction does not require dose adjustment of the preparation. There is no sufficient experience of using the preparation in children, therefore, it is not recommended to prescribe the preparation  to children.

Contraindications

During pregnancy and breastfeeding; hypersensitivity to rabeprazole or substituted benzimidazoles, during pregnancy and lactation.

Side effects

Usually well tolerated by patients. observed side effects are usually mild to moderate in severity, which quickly disappear.
The most common side effects (with a frequency of 5% or more) were headache, diarrhea and nausea, with a frequency of 2 to 5% - rhinitis, abdominal pain, asthenia, flatulence, pharyngitis, vomiting, back pain, dizziness, flu-like syndrome , infections, coughs, constipation and insomnia. With a frequency of less than 1%, skin rash, myalgia, chest pain, dry mouth, dyspepsia, increased nervous irritability, drowsiness, bronchitis, sinusitis, chills, belching, calf muscle cramps, urinary tract infections, arthralgia and fever were noted. In isolated cases, anorexia, gastritis, weight gain, depression, itching, disturbances in vision and taste, stomatitis, excessive sweating and leukocytosis were noted, however, the connection with Pariet was only established for headache, diarrhea, abdominal pain, asthenia, flatulence, skin rash and dry mouth.

special instructions

An improvement in symptoms after the use of parieta can also be observed in the presence of a malignant neoplasm of the stomach, therefore, before starting therapy, it is necessary to exclude such diseases.
Pariet is not recommended for use in children, as there is no experience with its use in this age group.
It is recommended to exercise caution in the early stages of therapy with Pariet in patients with severe renal impairment.
The safety of using rabeprazole during pregnancy has not been established. It has been experimentally established that the preparation can penetrate the placental barrier, therefore, the use of Pariet during pregnancy is contraindicated.
It is not known whether rabeprazole sodium is able to pass into breast milk; therefore, Pariet should not be given during breastfeeding.
Given the profile of side effects inherent in rabeprazole, Pariet should not adversely affect the ability to drive vehicles and work with potentially dangerous mechanisms. However, if drowsiness develops while taking the preparation, it is recommended to avoid such activities.

Interactions

The results of a study in healthy volunteers indicate that pariet does not enter into clinically significant interactions with other preparations metabolized by enzymes of the cyp450 system, such as warfarin, phenytoin, theophylline and diazepam.
The use of Pariet causes a pronounced and long-term decrease in the production of gastric acid. Consequently, it can interact with preparations, the absorption of which depends on the pH of the stomach contents, therefore, studies have been carried out to study the likelihood of such an interaction. Reception of Pariet caused a 33% decrease in plasma concentration of ketoconazole and a 22% increase in the minimum concentration of digoxin in healthy volunteers. Thus, in some patients, when these preparationsare taken together with Pariet, a dose adjustment may be required. In a special study, no interaction of Pariet with antacids was found. In addition, there was no clinically significant interaction of Pariet with food.
An in vitro study on human liver microsomes showed that sodium rabeprazole is metabolized by isoenzymes of the CYP450 system (CYP2C9 and CYP3A). Research results suggest that Pariet has a low ability to interact with other preparations; at the same time, its effect on the metabolism of cyclosporine is similar to the effect of other proton pump inhibitors.

Overdose

Doses up to 80 mg / day were well tolerated by patients. the specific antidote for pariet is unknown. in case of an overdose, it is necessary to carry out symptomatic and supportive therapy. the preparation is largely bound to blood plasma proteins, so dialysis is ineffective.

Storage conditions

At temperatures up to 25 ° C.

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