Rabelok - instructions for use, doses, side effects, contraindications

Excipients: mannitol 44.50 mg and 89.0 mg; magnesium oxide 40.0 mg and 80.0 mg: hypromellose 2.5 mg and 5.0 mg; cellulose microcrystalline 10.0 mg and 20.0 mg; starch 10.0 mg and 20.0 mg; carmellose 10.0 mg and 20.0 mg; talc 1.5 mg and 3.0 mg: magnesium stearate 3.0 mg and 6.0 mg; Silica colloidal dioxide 1.5 mg and 3.0 mg.

Sheath: hypromellose 4.75 mg and 9.5 mg; propylene glycol 0.75 mg and 1.5 mg;

Sour-insoluble shell: methacrylic acid and ethyl acrylate copolymer (type C) (1: 1) 6.975 mg, 13.95 mg; polysorbate 80 0.1045 mg and 0.209 mg; dibutyl phthalate 1.0450 mg and 2.090 mg; sodium hydroxide 0.0595 mgand 0.119 mg; ferric oxide of iron oxide 0.3915 mg and 0.783 mg; talc 2.815 mg and 5.63 mg; titanium dioxide 0.605 mg and 1.210 mg.

Description:

Tablets 10 mg

Round biconvex tablets, coated with a coating of light yellow to yellow, smooth on both sides.

Tablets 20 mg

Round biconvex tablets, coated with a coating of light yellow to yellow, smooth on both sides.

Pharmacotherapeutic group:a means of reducing 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:

Antiulcer from the group of proton inhibitorspump H + / K +ATP-az), metabolized in parietal cells of the stomach to active sulfonamide derivatives, which inactivate sulfhydryl groups of H + / K + -ATPase. It blocks the final stage of hydrochloric acid secretion, reducing the content of basal and stimulated secretion, regardless of the nature of the stimulus. It has high lipophilicity, easily penetrates into the parietal cells of the stomach and concentrates in them, providing a cytoprotective effect and increasing the secretion of bicarbonate.The antisecretory effect after oral administration of 20 mg occurs within 1 hour and reaches a maximum in 2-4 hours; oppression of basal and food-stimulated acid secretion at 23 hours after taking the first dose is 62 and 82% corresponding, 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 serum increases and returns to baseline levels during 1-2 ned after cancellation. Does not affect the central nervous system (CNS), cardiovascular and respiratory systems. Against the background of taking rabeprazole, stable changes in the morphological structure of enterochromaxin-like cells, in the degree of gastritis, in the frequency of atrophic gastritis, intestinal metaplasia, or the spread of infection Helicobacter pylori not detected.

Effect on the concentration of gastrin in the blood plasma. At the beginning of rabeprazole therapy, the concentration of gastrin in the blood plasma increases, which is a reflection of the inhibitory effect on the secretion of hydrochloric acid. The concentration of gastrin returns to baseline usually during 1-2 weeks after discontinuation of treatment.

Pharmacokinetics:

Absorption is high, the time to reach the maximum concentration (Tmax) - 3.5 hours. Maximum concentration (Сmах) and the area under the pharmacokinetic curve (AUC) in the blood plasma are linear in the range of doses from 10 to 40 mg. Metabolized in the liver with the participation of cytochrome isoenzymes CYP2C9 and CYP3A. Bioavailability - 52%, does not increase with multiple admission. The half-life (T1 / 2) is 0.7-1.5 hours, the clearance is 283+98 ml / min. In patients with hepatic insufficiency, the area under pharmacokinetic curve (AUC) increases by 2 rabehind. The half-elimination period T (1) - in 2-3 times. In elderly patients, the concentration in the blood plasma increases 2 times. Maximum concentration (Сmах) - by 60%. Relationship with baaplasma concentrations of 97%. To be displayed kidneys - 90% in the form of 2 metabolites: mercuric acid conjugate (M5) and carboxylic acid (M6); through the intestine - 10%.

Pharmacokinetics in special clinical cases

Renal insufficiency

In patients with stable renal insufficiency in the terminal stage, which require maintenance hemodialysis (creatinine clearance <5 ml / min / 1.73 m²) the removal of rabeprazole is similar to that of healthy volunteers. AUC and Сmах in these patients were approximately 35% lower than in healthy volunteers. Average, T1 / 2 Rabeprazole was 0.82 hours in healthy volunteers. 0.95 hours - in patients during hemodialysis and 3.6 hours after hemodialysis. The clearance of the drug in patients with diseases of nights requiring hemodialysis was approximately twice that of healthy volunteers.

Liver failure

Patients with chronic compensated cirrhosis are well tolerated rabeprazole in a dose of 20 mg once a day, although AUC doubled and Сmах increased by 50% compared to healthy volunteers.

Elderly patients

In elderly patients, the elimination of rabeprazole is somewhat slowed down. After 7 days of taking rabeprazole in a dose of 20 mg once a day in the elderly AUC was approximately twice as large, and Stach was increased by 60% compared to young healthy volunteers; There were no signs of cumulation with rabeprazole.

CYP2C19 polymorphism

In patients with delayed metabolism CYP2C19 after 7 days of taking rabeprazole at a dose of 20 mg per day AUC increases in 1,9 times, and the half-life is 1.6 times, in comparison with the same parameters in "fast metabolizers."while Сmах increases by 40%.

Indications:- Stomach ulcer in the stage of exacerbation and anastomosis ulcer;

- peptic ulcer of duodenum in the stage of exacerbation;

- erosive and ulcerative gastroesophageal reflux disease or reflux esophagitis;

- maintenance therapy of gastroesophageal reflux disease;

- non-erosive gastroesophageal reflux disease;

- Zolliiger-Elliope syndrome and other conditions characterized by pathological hypersecretion.

In the combination therapy:

- eradication Helicobacter pylori in patients with peptic ulcer of the stomach and duodenum or chronic gastritis.

Contraindications:

Individual hypersensitivity to rabeprazole, substituted benzimidazoles or to the accessory components of the drug, pregnancy, lactation, children's age until 12 years.

Carefully:

Severe renal failure, severe hepatic impairment, childhood

Pregnancy and lactation:

Contraindicated during pregnancy. If you need to use the drug during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Tablets are taken internally as a whole, without chewing or grinding. The time of day and food intake do not affect the activity of rabeprazole.

Adults.

With peptic ulcer in the acute stage and ulcer of anastomosis, it is recommended to take 10-20 mg once a day. Usually, the course of therapy is 6 weeks, in some cases the duration of treatment can be 6 pedel.

With duodenal ulcer in the acute stage, it is recommended to take 10-20 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 or reflux-esophagitis it is recommended to take 10-20 mg once a day. Duration of treatment is from 4 to 8 weeks. If necessary, the duration of treatment can be increased by 8 weeks.

With maintenance therapy gastroesophageal reflux disease is recommended to take 10-20 mg once a day. The duration of treatment depends on the patient's condition.

With non-erosive gastroesophageal reflux disease, it is recommended to take 10-20 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 should take the drug in a dose 10 mg once a day on request.

To treat the syndrome of Zolinger-Ellisop and other conditions characterized by pathological hypersecretion, the dose is selected individually. The initial dose is 60 mg per day, then the dose is increased and the drug is administered in a dose up to 100 mg per day with a single dose or 60 mg twice a day. Treatment should be conducted as clinical necessity. In some patients with Zollinger-Ellison syndrome, the duration of treatment with rabeprazole was up to one year.

For eradication Helicobacter pylori it is recommended to take 20 mg twice a day according to a certain scheme with the appropriate combination of antibiotics. Duration of treatment is 7 days.

Ppatients with renal insufficiency and elderly patients do not need dose adjustment. In patients with mild and moderate hepatic insufficiency, the concentration of rabeprazole in the blood is usually higher than in healthy patients. Care should be taken when administering the drug to patients with severe failure.

Children.

The safety and efficacy of rabeprazole in children aged 12 years and older is established for short-term 8 weeks) treatment of gastroesophageal reflux disease. The recommended dose for children aged 12 years and older is 20 mg once daily for up to 8 weeks. The safety and efficacy of rabeprazole for use in other indications is not established for pediatric patients.

Side effects:

To determine the incidence of side effects of the drug, the following classification is used: Often (>1/10); often (>1/100 and <1/10); infrequently (>1/100 and <1/100); rarely (> 1/10000 and, <1/1000); very rarely (< 1 /10000); frequency unknown (based on available of data establishing the frequency of occurrence is impossible).

From the hematopoiesis: rarely: neutropenia, leukopenia, thrombocytopenia. leukocytosis.

Allergic reactions: rarely: hypersensitivity (facial swelling, erythema), acute systemic allergic reactions.

From the nervous system: often: insomnia; infrequent: increased excitability; rarely: headache, dizziness, snotty, weakness, depression: frequency is unknown: confusion.

From the respiratory system: often: diarrhea, nausea, vomiting, abdominal pain, constipation, flatulence; infrequently: indigestion; dry mouth, belching; rarely: anorexia, gastritis, stomatitis, taste disorders, hepatitis, jaundice.

From the urinary system: not often: urinary tract infections; rarely interstitial nephritis.

From the skin: infrequent: rash, erythema; rarely: skin itching, increased sweating, bullous reactions; very rarely: polymorphic erythema, toxic epidermal necrolysis, Stephen's syndrome-Johnson.

Other: often: nonspecific pain, back pain, asthenia, flu-like syndrome; infrequently: myalgia, arthralgia, pain in the chest, spasms of gastrocnemius muscles, chills, fever, increased activity of "hepatic" enzymes; rarely: impaired vision, weight gain; frequency unknown: hyponatremia, peripheral edema, gynecomastia, hypomagnesemia (with prolonged use).

When taking proton pump inhibitors, an increased risk of fracture may occur.

Overdose:

Symptoms. Information on overdose is minimal.It was reported that rabeprazole was taken at a dose of 60 mg twice a day and 160 mg once. Side effects were minimal and did not require medical intervention.

Treatment. The specific antidote is unknown. Rabeprazole binds well to plasma proteins and is therefore poorly excreted in dialysis.

In case of an overdose, symptomatic treatment should be performed.

Interaction:

Slows the excretion of certain drugs metabolized in the liver by microsomal oxidation (diazepam, fenitoip, indirect anticoagulants). A joint appointment with rabeprazole sodium ketoconazole or itraconazole may lead to a significant decrease in the concentration of antifungal agents in blood plasma. It is not recommended joint use of rabeprazole with atanasavir, since the effects of atanasavir significantly decrease. Rabeprazole inhibits the metabolism of cyclosporine. Simultaneous administration of inhibitors of the purine pump and methotrexate may lead to an increase in the concentration and / or its metabolite of hydroxymetotransate and increase the period of excretion.

With the simultaneous use of rabeprazole and clarithromycin, indicators AUC and Сmах rabeprazole increased by 11% and 34%, respectively, a AUC and Сmах 14-hydroxyclarithromycin (the active metabolite of clarithromycin) increased by 42% and 46%, respectively. This increase in indicators was not clinically significant.

Special instructions:

Before and after treatment, endoscopic control is necessary to exclude malignant neoplasm, because treatment can mask the symptoms and delay correct diagnosis. The drug does not affect the function of the thyroid gland, the metabolism of carbohydrates, the concentration of thyroid hormone, cortisol, estrogen, testosterone, prolactin, cholecystokinin, secretin, glucagon, FSH, LH, renin, aldosterone and a growth hormone.

According to observational studies, proton pump inhibitor therapy may lead to an increased risk of osteoporotic fractures of the hip, wrist, spine. The risk of fractures was increased in patients who received high doses of proton pump inhibitors for a year or more.

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

During treatment should refrain from engaging in potentially hazardous activities,requiring increased concentration of attention (driving a car, working with mechanisms) and the speed of psychomotor reactions

Form release / dosage:

Tablets coated with enteric coating 10 mg and 20 mg.

Packaging:

14 tablets in a blister or in a contour non-cellular package made of foil and aluminum A1 / AI. By 1 or 2 blisters or contour non-jawed packaging of Aluminum foil A1 / A1 is placed in a pack of cardboard together with instructions for medical use.

Storage conditions:

In dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-002944

Date of registration:06.04.2015

The owner of the registration certificate:Cadil Pharmaceuticals Co., Ltd.Cadil Pharmaceuticals Co., Ltd. India

Manufacturer: & nbsp

CADILA PHARMACEUTICALS, Ltd. India

Representation: & nbspCADILA PHARMACEUTICALS LTD. CADILA PHARMACEUTICALS LTD. India

Information update date: & nbsp06.04.2015

Illustrated instructions

Instructions

Rabelok® (Rabeloc®)