Zulbex - instructions for use, dose, side effects, contraindications

Mannitol (E421) 18.50 mg / 37.00 mg, magnesium oxide light 30,00 mg / 60,00 mg, giprolase 2,625 mg / 5.25 mg, giprolase low-substituted 12.75 mg / 25.50 mg,

magnesium stearate 1.125 mg / 2.25 mg

Sheath (bonding layer):

ethyl cellulose 0.44 mg / 1.20 mg, magnesium light oxide 0.61 mg / 1.65 mg

Shell (enteric-soluble):

hypromellose phthalate 6,30 mg / 13.80 mg,

monoglycerides, diacetylated 0.64 mg / 1.40 mg,

talc 0.59 mg / 1.3 mg,

titanium dioxide (E171) 0.32 mg / 0.70 mg,

iron dye red oxide (E172) 0.017 mg / -,

dye iron oxide yellow (E172) - / 0.08 mg

Description:

Tablets 10 mg: round, biconvex tablets, covered with a film shell of orange-pink color, with a bevel.

Tablets of 20 mg: round, biconvex tablets, covered with a film coat of brownish-yellow color

Pharmacotherapeutic group:The iron of the stomach secretion is a reducing agent - a proton pump inhibitor.

ATX: & nbsp

A.02.B.C Proton pump inhibitors

A.02.B.C.04 Rabeprazole

Pharmacodynamics:

Rabeprazole belongs to the class of antisecretory drugs, substituted benzimidazoles, which do not possess anticholinergic or antihistamine (H₂) properties, and inhibit gastric secretion by inhibiting the enzyme H + / K + - ATPase (proton pump). The effect of the drug depends on the dose and leads to suppression of basal and stimulated secretion of hydrochloric acid in the stomach, regardless of the stimulating factors. Studies in animals have shown that rabeprazole quickly disappears from the plasma and the gastric mucosa. Being a weak ground, rabeprazole is quickly absorbed in all dosages and accumulates in the acidic environment of parietal cells of the stomach. Rabeprazole It is converted into a sulfenamide form by protonation and then interacts with the available cysteine molecules of the proton pump.

Antisecretory action: after ingestion of 20 mg of rabeprazole, the antisecretory effect begins to develop within 1 hour, reaching a maximum after 2-4 hours. The suppression of basal and food-stimulated hydrochloric acid secretion in the stomach after 23 hours after taking the first dose of rabeprazole is 69% and 82% and lasts up to 48 hours. The inhibitory effect of rabeprazole on the secretion of hydrochloric acid on receiving repeated doses increases somewhat, reaching an equilibrium state after 3 days. After the drug is discontinued, the secretory activity of the stomach is restored after 2 to 3 days.

In vitro it was found that rabeprazole has a bactericidal effect on Helicobacter pylori. Eradication Helicobacter pylori rabeprazole and antimicrobial drugs leads to a high degree of healing of mucosal lesions. According to the results of clinical studies, 20 mg rabeprazole 2 once a day in combination with two antibiotics, for example clarithromycin and amoxicillin or clarithromycin and metronidazole for 1 week allows you to achieve a level of eradication Helicobacter pylori more than 80% in patients with gastroduodenal ulcers. When choosing the right combination for eradication Helicobacter pylori should be guided by approved standards of treatment. In patients with persistent infection (in the presence of initially sensitive strains of microorganisms), it is necessary to consider the possibility of developing secondary resistance to antibacterial drugs when choosing a dosage regimen. Effect on serum gastrin: in clinical trials patients received rabeprazole in a dose of 10 or 20 mg once a day for up to 43 months. The concentration of gastrin in the serum increased in the first 2-8 weeks of admission, reflecting the inhibitory effect on the secretion of hydrochloric acid, and then remained stable while continuing therapy. The concentrations of gastrin returned to baseline values usually during 1-2 weeks after the abolition of therapy.

Samples of biopsy from the antral part and the bottom of the stomach, obtained from more than 500 patients who took rabeprazole or comparative treatment for up to 8 weeks, did not reveal any changes in the ECLcell and histological structure, the degree of gastritis, the incidence of atrophic gastritis, intestinal metaplasia, or the prevalence of infection H. pylori Ð ± Ð¾Ð »ÐμÐμ Ñ ‡ ÐμÐ¼ Ñƒ 250 Ð¿Ð ° Ñ † Ð¸ÐμÐ½Ñ,Ð¾Ð², Ð½Ð ° Ð ± Ð» ÑŽÐ'Ð ° Ð²ÑÐ¸Ñ ... Ñ Ñ Ð½Ð ° Ð¿Ñ € Ð¾Ñ,Ñ Ð¶ÐμÐ½Ð ¸Ð¸ 36 Ð¼ÐμÑ Ñ Ñ † ÐμÐ² Ñ,ÐμÑ € Ð ° Ð¿Ð¸Ð¸, Ð½Ðμ Ð ± Ñ <Ð »Ð¾ Ð²Ñ <Ñ Ð²Ð» ÐμÐ½Ð¾ Ð · Ð½Ð ° Ñ ‡ Ð¸Ð¼Ñ <Ñ ... Ð¸ See more about our products.

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Welcome to our website! Welcome to the website Weatherproof Ð½Ðμ Ð²Ñ Ñ,ÑƒÐ¿Ð ° ÐμÑ, Ð² ÐºÐ »Ð¸Ð½Ð¸Ñ ‡ ÐμÑ ÐºÐ¸ Ð · Ð½Ð ° Ñ ‡ Ð¸Ð¼Ð¾Ðμ Ð²Ð · Ð ° Ð¸Ð¼Ð¾Ð'ÐμÐ¹Ñ Ñ,Ð²Ð¸Ðμ Ñ Ð ° Ð¼Ð¾ÐºÑ Ð ¸Ñ † Ð¸Ð »Ð» Ð¸Ð½Ð¾Ð¼, Ð½Ðμ Ð¾ÐºÐ ° Ð · Ñ <Ð²Ð ° ÐμÑ, Ð½ÐμÐ³Ð ° Ñ,Ð¸Ð²Ð½Ð¾Ð³Ð¾ Ð²Ð »Ð¸Ñ Ð½Ð¸Ñ Ð½Ð ° ÐºÐ¾Ð½Ñ † ÐμÐ½Ñ,Ñ € Ð ° Ñ † WELCOME TO OUR SALES Ð »Ð ° Ð · Ð¼Ðμ ÐºÑ € Ð¾Ð²Ð¸ Ð¿Ñ € Ð¸ Ð¾Ð'Ð½Ð¾Ð²Ñ € ÐμÐ¼ÐμÐ½Ð½Ð¾Ð¼ Ð¿Ñ € Ð¸Ð¼ÐμÐ½ÐμÐ½Ð¸Ð¸ Ñ Ñ,Ð¸Ñ ... Ð¿Ñ € ÐμÐ¿Ð ° Ñ € Ð ° Ð Ð Ð Ð Ð Ð Ð ° ° ° ° ° ° Ð Ð H. pylori Welcome to our website. We will be pleased to hear from you.

Shrinkage:

Shallow depth of field: For more information, feel free to contact us, we will be pleased to answer your questions, please feel free to contact us. , Reliable, safe, reliable, (See the reference on the product).This form is due to the instability of rabeprazole in an acidic environment. Therefore, the absorption of rabeprazole begins only after the tablet has left the stomach. Suction fast; maximum concentration (Сmах) Rabeprazole in blood plasma is reached approximately in 3,5 hours after intake in a dose 20 mg. Stach and area under the curve "concentration-time" (AUC) have a linear character in the dose range from 10 mg to 40 mg. Absolute bioavailability of oral dose 20 mg (compared with intravenous administration) is approximately 52%, largely due to presystemic metabolism. With repeated use of bioavailability, apparently, does not increase. In healthy people, half-life (T 1/2) from the blood plasma is approximately 1 hour (0.7 to 1.5 hours), and the total clearance is 283 ± 98 ml / min. There is no clinically significant interaction associated with ingestion. Neither the food nor the time of taking the drug does not affect the absorption of rabeprazole.

Distribution: in man rabeprazole approximately 97% is associated with plasma proteins.

Metabolism and excretion: rabeprazole, like other representatives of the class of proton pump inhibitors, is metabolized in the liver, with the participation of cytochrome P450 (CYP450). Research in vitro with human liver microsomes showed that rabeprazole is metabolized by isoenzymes CYP450 (CYP2C19 and CYP3A4). In these studies rabeprazole in the expected plasma concentrations in humans did not suppress or stimulate CYP3A4. These results indicate that no interaction is expected between rabeprazole and cyclosporin. In humans, the main metabolites found in the plasma are thioether (M1) and carboxylic acid (M6), and sulfone (M2), desmethyl thioester (M4) and conjugate with mercapturic acid (M5) are determined in smaller quantities. Only the desmethyl metabolite (M3) has a low antisecretory activity, but it is not determined in plasma.

After a single oral intake of 20 mg,¹⁴C - labeled rabeprazole unchanged rabeprazole not excreted by the kidneys. Approximately 90% of the accepted dose is excreted by the kidneys in the form of two metabolites: a conjugate with mercapturic acid (M5) and carboxylic acid (M6), as well as in the form of two unknown metabolites. The rest of the injected drug is found in the contents of the intestine.

Floor: taking into account the corrections for height and body weight, there were no sex differences in pharmacokinetic parameters of rabeprazole in a dose 20 mg.

Impaired renal function: in patients with renal failure requiring hemodialysis (creatinine clearance less than 5 mL / min / 1.73 m2), the distribution of rabeprazole was similar to that in healthy volunteers. AUC and Сmах in such patients was approximately 35% lower than that in healthy

volunteers. Average T1/2, rabeprazole was 0,82 h in healthy volunteers, 0,95 h in patients with hemodialysis and 3.6 h after hemodialysis. CC of rabeprazole in patients with impaired renal function requiring maintenance hemodialysis was approximately twice as high as in healthy volunteers.

Impaired liver function: After a single application of rabeprazole at a dose of 20 mg in patients with mild or moderate liver disease, AUC, and in 2-3 times increased rabeprazole compared with healthy volunteers. However, after daily administration of 20 mg dose within 7 days AUC increased only in 1,5 times, and Stach - only in 1,2 times. T1/2, Rabeprazole in patients with impaired liver function was 12.3 hours compared with 2.1 hours in healthy volunteers. The pharmacodynamic response (pH control of the stomach) in the two groups was clinically comparable.

Elderly patients: in elderly patients the excretion of rabeprazole was slightly reduced.After using rabeprazole for 7 days in a daily dose of 20 mg AUC has increased approximately twice, and Stach increased by 60%, T1/2 was increased by 30% compared to healthy young volunteers. No evidence of rabeprazole accumulation was noted. Polymorphism CYP2C19: after ingestion of rabeprazole in a dose of 20 mg in people with delayed CYP2C19 - metabolism AUC and T1/2, were approximately 1.9 and 1.6 times higher than those in persons with active metabolism, whereas time as Сmах increased by only 40%.

Indications:

Stomach ulcer and duodenal ulcer in the stage of exacerbation;
Gastroesophageal reflux disease (GERD): erosive reflux-esophagitis (treatment), symptomatic treatment of GERD, including long-term maintenance therapy;
Zollinger-Ellison syndrome;
As part of complex therapy: eradication Helicobacter pylori in patients with gastric ulcer and 12the intestine or chronic gastritis;
Treatment and prevention of relapse of peptic ulcer associated with Helicobacter pylori

Contraindications:

Hypersensitivity to the active substance or auxiliary components of the drug, pregnancy, the period of breastfeeding, children's age (no experience of use).

Carefully:Severe kidney failure.

Pregnancy and lactation:

Application in pregnancy and during breastfeeding

Pregnancy

There is no data on the safety of rabeprazole during pregnancy in humans. Reproductive studies in rats and rabbits showed no signs of impaired fertility or the harmful effects of rabeprazole on the fetus.

Zulbecks is not used during pregnancy.

Lactation

It is not known whether the rabeprazole in the mother's milk, but is secreted into the milk of rats. Studies in women during lactation were not conducted.

If you need Zulbeks during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Inside, entirely, not liquid and not breaking.

Peptic ulcer of stomach and duodenum at the stage of exacerbation 20 mg once a day, in the morning.

In most patients, active ulcer of the duodenal ulcer heals within four weeks. However, some patients may need another 4 weeks to completely heal the ulcer. Active benign gastric ulcer in most patients heals within six weeks.However, in a small number of patients, it may take another six weeks for complete healing.

Gastroesophageal reflux disease (GERD): erosive reflux-esophagitis (treatment), symptomatic treatment of GERD

20 mg once a day for four to eight weeks.

With prolonged therapy, a maintenance dose of Zulbex® - 10-20 mg once a day, depending on the patient's response to treatment. Symptomatic treatment of GERD: 10 mg once a day in patients without esophagitis. If the symptoms can not be controlled within 4 weeks, an additional examination of the patient is necessary. After the improvement of the patient's condition, further control of the symptoms can be carried out by admission 10 mg 1 once a day, on demand.

Zollinger-Ellison Syndrome

The recommended starting dose for adults is 60 mg once a day. The dose can be increased to 120 mg per day, depending on the individual needs of the patient. You can appoint a daily dose of up to 100 mg once a day. A dose of 120 mg may require

fold intake, 60 mg twice a day. Therapy is performed as long as there are appropriate clinical indications.

Eradication H pylori in patients with peptic ulcer and duodenal ulcer or chronic gastritis: patients with I pylor, must undergo eradication therapy. The following combinations of preparations are recommended for 7 days:

The drug Zulbeks 20 mg twice a day + clarithromycin 500 mg twice a day and amoxicillin 1 g 2 times a day.

If eradication schemes require the use of drugs 1 once a day, the drug

Zulbeks must be taken in the morning, before breakfast; The time of day and food intake do not affect the activity of rabeprazole.

Impaired renal and / or liver function: correction of the dose of Zulbex is not required.

Childhood: Due to the lack of data on the efficacy and safety of rabeprazole Zulbecks is not used in children.

Side effects:

Classification of the frequency of development of side effects of the World Organization

Health (WHO):

very often>1/10

often from> 1/100 up to < 1/10

infrequently from> 1/1000 up to < 1/100

rarely from>1/10000 up to < 1/1000

very rarely from < 1/10000, including individual messages.

In each group, adverse events are listed in order of decreasing severity.

On the part of the hematopoiesis system:

- rarely: neutropenia, leukopenia, thrombocytopenia, leukocytosis;

From the immune system:

- often: reactions of increased sensitivity1;

Metabolic and nutritional disorders:

- Anorexia, weight gain;

-very rare: hyponatremia;

From the nervous system:

-frequently: headache, dizziness, insomnia;

-only: drowsiness, nervousness;

-only: depression;

-very rare: confusion;

From the sense organs:

- rarely: a vision disorder;

From the side of the heart - cardiovascular system:

-very rare: peripheral edema;

From the respiratory system:

-frequently: cough, pharyngitis, rhinitis;

-non-often: bronchitis, sinusitis;

From the digestive system:

-frequently: diarrhea, vomiting, nausea, abdominal pain, constipation, flatulence;

-nonly: dyspepsia, dryness of the oral mucosa, eructation;

-Seriously: gastritis, stomatitis, taste change, hepatitis, jaundice, hepatic encephalopathy; From the skin:

-nonly: rash, erythema;

-it: pruritus, sweating, bullous rash21

- very rarely: erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome;

From the musculoskeletal system:

-frequently: nonspecific pain, back pain;

-nonly: myalgia, calf muscle cramps, arthralgia;

From the urinary system:

- often: infections of the urinary tract;

- Interstitial nephritis;

On the part of the reproductive system:

-very rare: gynecomastia;

Laboratory indicators:

-only: increased activity of liver enzymes3 Other:

-frequently: asthenia, flu-like disease.

It includes facial swelling, lowering of blood pressure, dyspnea.
Erythema, bullous reactions and hypersensitivity reactions usually pass on their own after the drug is discontinued.
Rare reports of hepatic encephalopathy were obtained in patients with concomitant cirrhosis of the liver. When appointing the drug Zulbeks for the first time Care should be taken in patients with severe impairment of liver function.

Overdose:

The existing experience of a deliberate or accidental overdose of rabeprazole is limited. The maximum prescribed amount of the drug did not exceed 60 mg twice a day or 160 mg once a day. The effects were slightly pronounced, consistent with a well-known range of adverse reactions that occurred independently without any additional medical intervention. The specific antidote is unknown. Dialysis is ineffective.

Treatment: symptomatic.

Interaction:

Interaction with other drugs

Rabeprazole causes persistent and prolonged suppression of the secretion of hydrochloric acid in the stomach. There may be interaction with drugs, the absorption of which depends on the PH values. The simultaneous use of rabeprazole with ketoconazole or itraconazole may lead to a significant decrease in their concentration in the blood plasma, which may require a dose adjustment of these drugs.

Proton pump inhibitors, including rabeprazole, should not be used concomitantly with atazanavir.

Rabeprazole does not have a clinically significant interaction with amoxicillin and with other drugs metabolized by enzymes of the cytochrome system CYP450, such as warfarin, phenytoin, theophylline and diazepam.

Rabeprazole slows the excretion of certain drugs metabolized in the liver by microsomal oxidation (diazepam, phenytoin, indirect anticoagulants).

Concentrations of rabeprazole and the active metabolite of clarithromycin in plasma with simultaneous admission are increased by 24 % and 50 %, respectively.Reduces the concentration of ketoconazole by 33%, digoxin by 22%.

Special instructions:

Reducing the severity of symptoms on the background of therapy with Zulbeks does not exclude the presence of malignant tumors in the stomach or esophagus, therefore, before the start of therapy it is necessary to conduct a checkup, in order to exclude the growth of the gastrointestinal tract.

Patients receiving long-term therapy with Zulbecks (especially more than one year) should undergo a regular examination.

It is impossible to exclude the risk of cross-reactions with other inhibitors of the proton pump or with substituted benzoimidazoles.

The patient must be warned that the pill must be swallowed whole, not chewing and not breaking.

The drug Zulbeks is not recommended for children; experience in the use of the drug in this group of patients is absent.

There are reports of post-marketing research on the development of blood dyscrasias (cases of thrombocytopenia and neutropenia) on the background of the use of rabeprazole. In most cases, when it was not possible to find out the alternative causes of these conditions, they did not give complications and passed after the abolition of rabeprazole.

Against the background of the use of Zulbex®, a change in the activity of liver enzymes that occur after the drug has been withdrawn is possible.

In a study in patients with mild or moderate hepatic impairment, there were no significant safety problems with the use of rabeprazole, compared to the control group of healthy patients corresponding to sex and age. Due to the lack of clinical data on the use of rabeprazole in patients with severe liver dysfunction, caution should be exercised when using Zulbex in this group of patients

Effect on the ability to drive transp. cf. and fur:

Based on the properties of rabeprazole, it is unlikely that the Zulbex product may interfere with the ability to drive vehicles or affect the operation of technical devices. In case of side effects (drowsiness, dizziness, confusion), you should give up driving and work, which requires an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Intestine-soluble tablets shell, 10 mg and 20 mg.

Packaging:

For 14 or 15 tablets per blister of combined material OPA / Al / PVC and aluminum foil.

By 1, 2 or 4 blisters together with instructions for use are

a pack of cardboard.

Storage conditions:At a temperature not exceeding 30 degrees.

In a place inaccessible to children.

Shelf life:2 years.

Terms of leave from pharmacies:On prescription

Registration number:LP-000944

Date of registration:18.10.2011

The owner of the registration certificate:KRKA-RUS, LLC KRKA-RUS, LLC Russia

Manufacturer: & nbsp

KRKA, d.d. Slovenia

Representation: & nbspKRKA KRKA Slovenia

Information update date: & nbsp03.12.2014

Illustrated instructions

Instructions

Zulbex® (Zulbex® )