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

Auxiliary Ingredients: magnesium oxide 50 mg, mannitol 17.5 mg, corn starch 2.5 mg, povidone-KZO 1.5 mg, low-substituted giprolase 16 mg, sodium stearyl fumarate 2 mg.

Sheath: cellulose 11.25 mg, titanium dioxide 1 mg, ferric oxide red 0.1 mg.

Dosage of 20 mg:

Active Ingredient: Rabeprazole sodium - 20 mg.

Auxiliary Ingredients: magnesium oxide 69 mg, mannitol 40 mg, corn starch 2.5 mg, povidone-KZO 1.5 mg, low-substituted giprolase 24 mg, sodium stearyl fumarate 2 mg.

Sheath: cellulose 18 mg, titanium dioxide 1.6 mg, iron dye oxide yellow 0.16 mg

Description:

Dosage of 10 mg:

round biconvex tablets, coated with a coat of light pink to reddish-pink.

Hbut transverse cut the core of white or white with a yellowish hue of color.

Dosage of 20 mg:

round biconvex tablets, coated with a coating of light yellow to yellow.

On the cross-section the nucleus is white or white with a yellowish tint of color.

Pharmacotherapeutic group:a drug that reduces the secretion of the glands of the stomach - the proton pump inhibitor

ATX: & nbsp

A.02.B.C Proton pump inhibitors

A.02.B.C.04 Rabeprazole

Pharmacodynamics:

An anti-ulcer agent from the proton pump inhibitor group (H + / K + -ATPase) is metabolized in parietal cells of the stomach to active sulfonamide derivatives that inactivate the sulfhydryl groups of H + / K + -ATPase.

It blocks the final stage of the secretion of hydrochloric acid, reducing the content of basal and stimulated secretion, regardless of the nature of the stimulus.

It has a high lipophilicity, easily penetrates into the parietal cells of the stomach and concentrates in them, providing a cytoprotective effect.The antisecretory effect after oral administration of 20 mg occurs within 1 hour and reaches a maximum after 2-4 hours; inhibition of basal and stimulated food secretion of acid 23 hours after the first dose is 62% and 82%, respectively; the duration of action is 48 hours. After the end of the reception, the secretory activity is normalized within 2-3 days.

In the first 2-8 weeks of therapy, the concentration of gastrin in the blood serum increases and returns to baseline levels within 1-2 weeks after drug discontinuation. Does not affect the central nervous system, cardiovascular and respiratory systems.

Pharmacokinetics:

Absorption occurs in the small intestine (due to the presence of an acid-resistant enteric-insoluble coat) high, the time to reach the maximum concentration is 3.5 hours. The values of the maximum concentration (Сmах) and the area under the curve "concentration of active substance - time" (AUC) are linear in the dose range of 10 to 40 mg. Metabolized in the liver with the participation of cytochrome P-450 isoenzymes CYP2C19 and CYP3A4. Bioavailability - 52%, does not increase with multiple admission. Half-life (T1 / 2) - 0,7-1,5 h, clearance - 283 ± 98 ml / min.

In patients with chronic hepatic insufficiency of mild or moderate degree after a single dose AUC increases 2 times, T1/2 - 2-3 times. After taking 20 mg of rabeprazole for 7 days AUC increases by 1.5 times, T1 / 2 - by 1.2 times.

In patients with stable terminal stage of renal failure requiring hemodialysis (creatinine clearance less than 5 ml / min / 1.73 m2), the distribution of rabeprazole sodium is close to that in healthy individuals.

In elderly patients after taking rabeprazole for 7 days AUC in 2 times more, Сmах - 60% more than in young people.

The connection with plasma proteins is 97%.

It is excreted by the kidneys - 90% in the form of two metabolites: a conjugate of mercapturic acid (M5) and carboxylic acid (MB); intestine - 10%.

In patients with delayed metabolism CYP2C19 after 7 days of taking rabeprazole at a dose of 20 mg per day AUC increases by 1.9 times, and the half-life period is 1.6 times as compared with the same parameters for "fast metabolizers ", while Сmах increases by 40%.

Indications:

Stomach ulcer in the stage of exacerbation and ulcer of anastomosis;

Peptic ulcer of duodenum in the stage of exacerbation;

Erosive and ulcerative gastroesophageal reflux disease or reflux esophagitis;

Supportive therapy

gastroesophageal reflux disease; Non-erosive gastroesophageal

reflux disease;

Zollinger-Ellison syndrome and other conditions characterized by

pathological hypersecretion;

In combination with appropriate antibiotic therapy for Helicobacter pilory in patients with peptic ulcer.

Contraindications:

Hypersensitivity to rabeprazole, substituted benzimidazoles or other auxiliary components of the formulation; pregnancy; lactation period; children's age (up to 12 years).

Carefully:Severe hepatic insufficiency, severe renal failure.

Pregnancy and lactation:

Rabeprazole should not be given to pregnant women (there is no safety data for the use of rabeprazole during pregnancy). For the duration of treatment, breastfeeding should be discontinued. It is not known whether rabeprazole with breast milk. Appropriate studies in lactating women were not conducted.

Dosing and Administration:

Tablets of the drug Khyrabesol can not chew or grind. Tablets should be swallowed whole.It has been established that neither the time of day nor the intake of food affects the activity of rabeprazole.

With gastric ulcer in the stage exacerbation and ulcer of anastomosis

it is recommended to take inside 10 mg or 20 mg once a day. Usually, the cure comes after 6 weeks of therapy, but in some cases the duration of treatment can be increased by another 6 weeks.

With duodenal ulcer in the acute stage it is recommended to take inside 20 mg once a day. In some cases, the therapeutic effect occurs when taking 10 mg once a day. Duration of treatment is from 2 to 4 weeks. If necessary, the duration of treatment can be increased by another 4 weeks.

In the treatment of erosive gastroesophageal reflux disease (GERD) or reflux esophagitis it is recommended to take inside 10 mg or 20 mg once a day. Duration of treatment is from 4 to 8 weeks. If necessary, the duration of treatment can be increased by another 8 weeks.

When maintenance therapy gastroesophageal reflux disease (GERD) it is recommended to take inside 10 mg or 20 mg once a day.The duration of treatment depends on the patient's condition.

With non-erosive gastroesophageal reflux disease (NERD) without esophagitis it is recommended to take inside 10 mg or 20 mg once a day.

If after four weeks of treatment the symptoms do not disappear, an additional study of the patient should be carried out. After relief of symptoms to prevent their subsequent occurrence, the drug should be taken orally at a dose of 10 mg once a day on demand.

To treat the syndrome of Zollingea-Alison and other conditions characterized by pathological hypersecretion, dose select individually. The initial dose is 60 mg per day, then the dose is increased and the drug is given in a dose of up to 100 mg per day with a single dose or 60 mg twice a day. For some patients, fractional dosing of the drug is preferred. Treatment should continue as clinical need arises. In some patients with Zollinger-Alison syndrome, the duration of treatment with rabeprazole is up to one year.

DFor the treatment of ulcerative duodenum guts or chronic gastritis, associated with H. infection. pylori, a course of treatment of 7 days with one of the following combinations of drugs is recommended:

Hyabrezole 20 mg twice a day + clarithromycin 500 mg twice a day and amoxicillin by 1g. 2 times a day.

Hyabrezole 20 mg twice a day + clarithromycin 500 mg twice a day and metronidazole 400 mg 2 times a day.

Patients with renal and hepatic insufficiency Dose adjustments in patients with renal insufficiency are not required. In patients with mild and moderate hepatic insufficiency, the concentration of rabeprazole in the blood is usually higher than in healthy patients.

When administering the drug, hirabesol, patients with severe hepatic impairment should be observedgive caution.

Elderly patients Correction of the dose is not required.

Children

The safety and efficacy of rabeprazole 20 mg for short-term (up to 8 weeks) treatment of GERD in children aged 12 years or more is confirmed by extrapolating the results of adequate and well-controlled studies that support the efficacy of rabeprazole for adults and safety studies and pharmacokinetics for pediatric patients.The recommended dose for children aged 12 years and over is 20 mg once a day for up to 8 weeks.

The safety and efficacy of rabeprazole for the treatment of GERD in children under the age of 12 years has not been established. The safety and efficacy of rabeprazole for use in other indications is not established for pediatric patients.

Side effects:

Based on the experience of clinical trials, it can be concluded that rabeprazole usually well tolerated by patients. Side effects are generally mild or moderate and of a transient nature.

When taking rabeprazole in clinical trials, the following side effects were noted: headache, abdominal pain, diarrhea, flatulence, constipation, dry mouth, dizziness, rash, peripheral edema.

During the post-marketing application of rabeprazole, the following side effects were reported: elevation of the level of hepatic enzymes, rarely - hepatitis and jaundice. Patients with cirrhosis of the liver rarely reported the development of hepatic encephalopathy. Also, in rare cases, thrombocytopenia, neutropenia, leukopenia, bullous eruptions, urticaria, acute systemic allergic reactions, myalgia, arthralgia, hypomagnesemia were noted.Very rarely reported on the development of interstitial nephritis, gynecomastia, erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome. According to post-marketing surveillance data, an increase in the risk of fracture is possible with the intake of proton pump inhibitors (see section "Special instructions")

Overdose:

Symptoms:

Data on intentional or accidental overdose are minimal. There were no cases of severe overdose with rabeprazole.

Treatment:

The specific antidote for rabeprazole is unknown. Rabeprazole binds well to plasma proteins, and therefore is poorly excreted by dialysis. In case of an overdose, symptomatic and supportive treatment should be performed.

Interaction:

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

Reduces the concentration of ketoconazole by 33%, digoxin by 22%.

Does not interact with liquid antacids. Compatible with drugs metabolized by the system CYP450 (warfarin, phenytoin, theophylline, diazepam).

Special instructions:

The patient's response to rabeprazole therapy does not exclude the presence of malignant neoplasms in the stomach. Tablets of the preparation Khyrabesol can not be chewed or crushed. Tablets should be swallowed whole. It has been established that neither the time of day nor the intake of food affects the activity of rabeprazole. In a special study in patients with mild or moderate liver function abnormalities, there was no significant difference in the frequency of side effects of rabeprazole from that of the healthy individuals selected by sex and age, but in spite of this, caution should be exercised in the first appointment to patients with severe impaired hepatic function .

Patients with impaired renal or hepatic function are not required to adjust the dose of the drug Khyrabezol. AUC Rabeprazole in patients with severe impairment of liver function is approximately twice as high as in healthy patients.

Hypomagnesemia

When treating proton pump inhibitors for at least 3 months, in rare cases, cases of symptomatic or asymptomatic hypomagnesemia were noted. In most cases, these reports were received one year after the therapy.Serious side effects were tetany, arrhythmia and convulsions. Most patients required treatment of hypomagnesemia, which included the replacement of magnesium and the withdrawal of therapy with proton pump inhibitors. In patients who will receive long-term treatment or who take proton pump inhibitors with drugs such as digoxin or drugs that can cause hypomagnesemia (eg, diuretics), health workers should monitor the magnesium level before starting treatment with proton pump inhibitors and during treatment.

Fractures

According to observational studies, it can be assumed that therapy with proton pump inhibitors can lead to an increase in the risk associated with osteoporosis of hip, wrist, spine fractures. The risk of fractures was increased in patients taking high doses of proton pump inhibitors for a year or more.

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

In the case of the appearance of drowsiness during the treatment should be abandoned from driving and other activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:tablets coated with enteric film coating of 10 mg and 20 mg.

Packaging:

For pharmacies:

10, 14, 15 tablets in Al / Al blister or in Al / Al strip.

1 or 10 strips / blisters for 10 tablets, 1 or 2 strips / blisters for 14 tablets, 1, 2 or 10 strips / blisters for 15 tablets together with instructions for use in a pack of cardboard.

1 strip / blister for 14 or 15 tablets together with instructions for use in a pack of cardboard with a valve and perforations protected with a PVC film on the inside of the pack (7 perforations in the form of a circle).

For hospitals:

100, 500, 1000 tablets in a package of polyethylene.

Package with instructions for use in a can of high-density polyethylene. A label is attached to the jar.

Storage conditions:

In a dry, dark place at a temperature of 8 ° C to 25 ° C. Keep out of the reach of children

Shelf life:2 years. Do not use at the expiration date indicated on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-001479

Date of registration:06.02.2012

The owner of the registration certificate:Highgans Laboratories Pvt. Ltd.Highgans Laboratories Pvt. Ltd. India

Manufacturer: & nbsp

HIGLANCE LABORATORIES Pvt. Ltd. India

Representation: & nbspHAYGLANCE LABORATORY HAYGLANCE LABORATORY India

Information update date: & nbsp13.03.2014

Illustrated instructions

Instructions

Hirabezol® (Hirabezol®)