Producer: Torrent Pharmaceuticals Ltd (Torrent Pharmasyyutikals Ltd) India
Code of automatic telephone exchange: A02BC04
Release form: Firm dosage forms. Tablets.
General characteristics. Structure:
Active ingredient: 10 mg or 20 mg of a rabeprazol of sodium.
Excipients: magnesium oxide easy, mannitol (Е 421), кросповидон (XL-10), sodium hydroxide, K-30 povidone, magnesium stearate, silicon dioxide colloid anhydrous.
Coverings (soil): gidroksipropilmetiltsellyuloza, silicon dioxide colloid anhydrous, ethyl cellulose, talc, diethyl phthalate.
Covering (kishkovorozchiyena): gidroksipropilmetiltsellyuloza phthalate, titanium dioxide (Е 171), ferrous oxide yellow (Е 172), talc, diethyl phthalate.
Pharmacodynamics. Rabeprazol belongs to a class of anti-secretory connections which in the chemical relation are the replaced benzimidazoles. Drug suppresses secretion of gastric acid by specific oppression of enzyme of N/K-ATP-ase on the secretory surface of covering cells of a stomach. This fermental system is considered the acid (proton) pump, and, thus, рабепразол is classified as inhibitor of the proton pump of a stomach which blocks a final stage of production of acid. Rabeprazol turns into an active sulfonam_dna a form by протонування and, thus, reacts with the available remains of cysteine of the proton pump.
After oral administration of a rabeprazol the anti-secretory effect is observed in 1 hour and reaches a maximum in 2-4 hours. The effect of suppression of basal function and stimulation by food of secretion of acid in 23 hours after reception of the first dose of a rabeprazol made 62 and 82% respectively, and duration of this effect reached 48 hours. Efficiency of a rabeprazol on acid secretion oppression amplifies a little in the course of daily reception of 1 tablet (20 mg), but stable oppression of secretion is reached in 3 days after the beginning of reception of this drug. After completion of use of a rabeprazol secretory activity is normalized within 2-3 days.
After reception of 10 mg or 20 mg of a rabeprazol of 1 times a day within 12 months in the first 2 - 8 weeks of therapy concentration of gastrin increases in serum that leads to acid secretion oppression. Concentration of gastrin is returned to initial level, as a rule, within 1-2 weeks after the treatment termination.
Still there are no data on system effects from the central nervous system, cardiovascular and respiratory systems which would be caused by reception of a rabeprazol.
Pharmacokinetics. Absorption. Veloz – tablets, coated which is dissolved in intestines. Rabeprazol is quickly absorbed from intestines. Peak concentration of a rabeprazol in a blood plasma are reached approximately in 3,5 h after reception of a dose of 20 mg. Peak concentration in a blood plasma (Smakh) and the area under curve (AUC) of a rabeprazol have linear character in the range of doses from 10 to 40 mg. Absolute bioavailability after oral administration of 20 mg (in comparison with intravenous administration) makes about 52% substantially for metabolism of the first passing. Besides, bioavailability does not increase at multiple dose of a rabeprazol of sodium. Plasma elimination half-life of blood makes about 1 hour (from 0,7 to 1,5 hours), and the total clearance makes 283±98 ml/min. according to estimates.
The food and time of reception within a day do not influence absorption of a rabeprazol of sodium.
Distribution. At the person extent of linkng of a rabeprazol of sodium with proteins of a blood plasma makes about 97%.
Metabolism and excretion. At the person the main metabolites which are present at a blood plasma is тіоефір (MI) and carboxylic acid (M6), and minor metabolites, present at low concentration, are presented by sulphone (Sq.m), dimetilt_oyef_ry (M4) and a conjugate меркаптурово ї acid (M5). Only the dimethyl metabolite (MZ) has insignificant anti-secretory activity, however it is not present at a blood plasma.
Indications to use:
- active round ulcer of a duodenum,
- active benign stomach ulcer,
- erosive or ulcer gastroesophageal reflux disease (GERB),
- prolonged treatment of a gastroesophageal reflux disease (maintenance therapy of GERB),
- a symptomatic treatment of a gastroesophageal reflux disease from moderated to very heavy degree (a symptomatic treatment of GERB),
- Zollingera-Ellison's syndrome,
- in a combination with the corresponding antibacterial therapeutic schemes for an eradikation of Helicobacter pylori (H. pylori) at patients with a round ulcer of a stomach and duodenum.
Route of administration and doses:
Adults, including patients of advanced age. Active round ulcer of a duodenum and active benign stomach ulcer: the recommended dose at these diseases makes 20 mg of 1 times a day in the morning.
At most of patients with an active round ulcer of a duodenum time necessary for healing of an ulcer makes up to 4 weeks. It should be noted, however, that some patients for recovery should accept Veloz in addition within 4 more weeks. At most of patients healing happens to active benign stomach ulcer in 6 weeks, but to some patients, insensitive to treatment, for healing of ulcers it is necessary to accept Veloz in addition within 6 more weeks.
Erosive or ulcer gastroesophageal reflux disease: the recommended dose at these diseases makes 20 mg of 1 times a day within 4-8 weeks.
Prolonged treatment of a gastroesophageal reflux disease (maintenance therapy of GERB): it is possible to apply maintenance doses of Veloso of 10 mg or 20 mg of 1 times a day to prolonged treatment (depending on efficiency of treatment).
Symptomatic treatment of GERB from moderated to very heavy degree: to patients without esophagitis Veloz appoint in a dose 10 mg of 1 times a day. If after 4 weeks of treatment symptoms do not disappear, it is necessary to conduct additional examination of the patient. As soon as symptoms disappear, further control of symptoms can be reached use of the mode "upon the demand of": to apply 10 mg of 1 times a day as necessary.
Zollingera-Ellison's syndrome: the dose is selected individually. An initial dose – 60 mg a day. It is possible to apply a single dose to 100 mg a day. In case of need the dose is raised and appoint drug in a dose of 120 mg a day – on 60 mg 2 times a day. Treatment is continued so much how many it is clinically necessary. Some patients with Zollingera-Ellison's syndrome received treatments rabeprazoly sodium during 1 year.
Eradikation N. pylori: to patients with N. of pylori, it is necessary to apply the corresponding combinations of Veloso with antibiotics. Appointment within 7 days is recommended:
Veloz of 20 mg 2 times a day кларитромицин 500 mg 2 times a day and amoxicillin of 1 g 2 times a day. According to indications, demanding reception of 1 times a day, Veloz a pill should be taken in the morning before meal. Though there is no inclusion in the first half of day, food did not show influence on action of a rabeprazol of sodium, this mode more favorable for treatment. Veloz Tabletki it is impossible to chew or split up, it is necessary to swallow of them entirely.
Renal failure and liver. Patients with renal failures or a liver do not demand dose adjustment of Veloso. Veloso's use at treatment of patients with heavy abnormal liver functions is in more detail considered in the section "Features of Use".
Features of use:
Use during pregnancy or feeding by a breast. Pregnancy
Use of drug during pregnancy is contraindicated. Disturbance of fertility or the harm for a fruit connected using a rabeprazol of sodium was not revealed, however it was observed insignificant placental penetrations.
Feeding by a breast. It is unknown whether gets рабепразол sodium into breast milk at women therefore Veloz do not apply during feeding by a breast.
Children. Drug is not appointed to children as there is no sufficient experience of its use in this age group of patients for today.
Features of use. It is necessary to be careful at purpose of a rabeprazol to patients with the known hypersensitivity to drugs. The risk of cross hypersensitivity with other inhibitors of a proton pomp or the replaced benzimidazoles is not excluded.
Use by patients of advanced age. Veloz is metabolized only in a liver. As with age physiological function of a liver can be weakened, patients of advanced age can have side reactions. Therefore for patients of advanced age it is necessary to look after and adhere to recommendations concerning a dosage and duration of treatment.
Symptomatic improvement in response to therapy rabeprazoly can happen also in the presence of a malignant new growth of a stomach therefore before therapy by Veloz it is necessary to exclude a possibility of existence of tumors.
Patients who take a long course of treatment (especially those that more than one year are treated) should be inspected regularly.
Patients should be warned that Veloz tablets cannot be chewed or split up, and it is necessary to swallow whole.
Pathological changes of blood (thrombocytopenia and neutropenia) were noted. In most cases other etiology was not found, changes of blood were uncomplicated and disappeared after phase-out of a rabeprazol.
Deviations of liver enzymes from norm were observed. In most cases other etiology was not found, disturbances were uncomplicated and disappeared after phase-out of a rabeprazol.
At patients with easy or moderate abnormal liver functions the considerable difference of frequency of side effects at Veloso's reception was not observed in comparison with that in control group of the corresponding gender and age. The doctor should be careful at purpose of drug Veloz at early stages of therapy to patients with heavy abnormal liver functions as there are no clinical data on drug use to patients of this group.
During treatment by Veloz it is recommended to hold hematologic and biochemical testings periodically.
Simultaneous use of an atazanavir and Veloso it is not recommended (see the section "Interaction with Medicines and Other Types of Interactions").
Treatment by inhibitors of a proton pomp, including Veloz, increases risk of developing of gastrointestinal infections, such as Salmonella, Campylobacter and Clostridium difficile (see the section "Pharmacodynamics").
Hypomagnesiemia. The hypomagnesiemia (symptomatic or symptomless) can arise at patients who accept inhibitors of a proton pomp within three months and more, and is shown by such symptoms as arrhythmia, spasms, a tetany. Treatment of a hypomagnesiemia demanded the termination of reception of IPP and purpose of corrective replacement therapy from most of patients magnesium drugs. At patients at prolonged simultaneous treatment with digoxin or drugs which lead to a hypomagnesiemia (for example with diuretics) it is necessary to control magnesium level in blood prior to the beginning of and during treatment.
Function of a thyroid gland. It is recommended to monitor function of a thyroid gland during treatment by Veloz.
Features of carrying out respiratory tests. Results S-ureaznikh of respiratory tests can be hibnonegativny during reception of inhibitors of a proton pomp, such as рабепразол, and antibiotics, such as amoxicillin, кларитромицин and metronidazole. Therefore for Helicobacter pylori existence definition respiratory tests should be carried out not earlier than in 4 weeks after the end of treatment by such drugs.
Risk of changes. Assume that inhibitors of a proton pomp increase risk of osteoporozozalezhny fractures of hip, wrist and vertebrae. The risk of changes increased at patients who a long time (more than 1 year) received high doses of IPP.
As a maintenance therapy at a reflux esophagitis Veloz patients can appoint only with palindromias. It is not necessary to appoint Veloz that who does not need a maintenance therapy. It is recommended to stop treatment on condition of improvement of the state of health by means of a diet, alcohol intake restriction, and also in case of lack of aggravations throughout a long time. Careful inspection, namely periodic endoscopy, is shown at a maintenance therapy.
Treatment of a neerozivny reflux disease is shown to patients who have the repeating reflux symptoms, in particular heartburn and an acid reflux (around two weekly). Veloso's use can hide symptoms of a malignant tumor (for example, a carcinoma of the stomach or intestines) and other diseases of digestive tract. Therefore it is necessary to exclude existence of these diseases before Veloso's appointment.
On condition of Veloso's appointment the patient with a reflux disease without erosion to the doctor should be convinced of efficiency of treatment after 2 weeks of use of drug. If symptoms did not disappear, there is a probability that the reflux disease is not the reason of their emergence. In that case the doctor has to apply other method of treatment.
If Veloz appoint for the purpose of Helicobacter pylori eradikation, it is important to pay attention to the contraindications, features of use, clinically significant side reactions and other precautions specified in instructions for a medical use of other medicines applied for the purpose of an eradikation.
Ability to influence speed of response at control of motor transport or work with other mechanisms. Considering an inherent profile of side reactions of a rabeprazol, it is possible to consider that drug should not influence negatively on driving by motor transport and work with potentially dangerous mechanisms. However in case of drowsiness it is recommended to refrain from driving or work with other mechanisms.
The headache, diarrhea, abdominal pain, adynamy, meteorism, rash and dryness in a mouth were the most frequent side reactions about which it was reported. Side effects which were observed were mostly insignificant, moderate and quickly passed.
Infections and invasions: infections.
From immune system: hypersensitivity (including urticaria, a face edema, arterial hypotension and диспноэ, the erythema, violent reactions and acute system allergic reactions, usually disappear after the treatment termination).
Mental disorders: sleeplessness, nervousness, depression, confusion of consciousness.
From a nervous system: a headache, drowsiness, dizziness, weakness in extremities, numbness of extremities, a hypesthesia, decrease in force of compression of a brush, disturbance of the speech, a disorientation, a delirium, a coma.
From organs of sight: visual disturbances, increase in intraocular pressure.
Vascular frustration: peripheral hypostasis, arterial hypertension, palpitation.
From a digestive tract: diarrhea, vomiting, nausea, abdominal pain, a lock, a meteorism, feeling of overflow and weight in a stomach, candidiasis, dyspepsia, dryness in a mouth, an eructation, gastritis, stomatitis, disturbance of feeling of taste, enteritis, an esophagitis, a cheilitis, heartburn, hemorrhoids.
From skin and hypodermic fabrics: rash, an erythema (violent reactions and acute system allergic reactions, usually disappear after the treatment termination), an itch, perspiration, violent reactions, a multiformny erythema, the toxic epidermal necrolysis (TEN), Stephens-Johnson's syndrome.
From reproductive system: gynecomastia, strengthening of an erection.
Laboratory indicators: increase in level of liver enzymes (ALT, nuclear heating plant), LDG, gamma глутамилтрансферазы, alkaline phosphatase, general bilirubin, increase in body weight, proteinuria, increase in level of the general cholesterol, triglycerides, urea nitrogen, increase in the TSG, KFK level, uric acid, urine glucose, giperammoniyemiya.
In rare instances hepatic encephalopathy was observed at patients with cirrhosis. It is necessary to be careful at purpose of treatment drug Veloz to patients with heavy abnormal liver functions (see the section "Features of Use").
Side reactions which have clinical value:
- shock and anaphylactic reactions,
- pancytopenia, leukopenia, agranulocytosis and hemolitic anemia,
- fulminantny form of hepatitis, abnormal liver function, jaundice,
- intersticial pneumonia,
- toxic epidermal necrolysis, St_venasa-Johnson's syndrome, multiformny erythema,
- acute renal failure, intersticial nephrite,
Side reactions which have clinical value and are inherent to inhibitors of a proton pomp:
- vision disorders,
- Quincke's disease, bronchial spasm,
- confusion of consciousness.
Interaction with other medicines:
CYP-450 system. Rabeprazol of sodium is metabolized by system of CYP-450 liver enzymes, namely CYP2C19 and CYP3A4.
Rabeprazol of sodium has no pharmacokinetic or clinically significant interactions with warfarin, Phenytoinum, theophylline or diazepam, each of which is metabolized by CYP-450.
The interactions caused by oppression of secretion of gastric acid. Sodium рабепразол causes strong and long decrease in production of gastric acid. Thus, рабепразол in principle can interact with drugs which absorption depends on an indicator рН gastric contents. Simultaneous use of a rabeprazol of sodium and a ketokonazol or itrakonazol can lead to decrease in concentration of the last in plasma, and use with digoxin can lead to increase in concentration of the last. Therefore certain patients who use the specified drugs together with Veloz should be under observation of the doctor for definition of need of dose adjustment.
Antacids. At patients who along with rabeprazoly sodium accepted antacids interaction of drug with antacids, such as aluminum or magnesium hydroxide was not observed.
Atazanavir. Simultaneous use of an atazanavir of 300 mg / ритонавира 100 mg with omeprazoly () or an atazanavira of 400 mg with lanzoprazoly (60 mg of 1 times a day) led 40 mg of 1 times a day to considerable decrease in exposure of an atazanavir. Absorption of an atazanavir depends from рН. Similar results of use of other inhibitors of a proton pomp are expected. Inhibitors of a proton pomp, including рабепразол, should not be applied in a combination with atazanaviry (see the section "Features of Use").
Food. The use of food with the low content of fats does not influence absorption of a rabeprazol of sodium. Reception of a rabeprazol of sodium with greasy food can detain absorption for 4 hours and more, however the maximum concentration and level of absorption remain invariable.
Cyclosporine. Rabeprazol of sodium inhibits cyclosporine metabolism. This level of inhibition similar to inhibition level omeprazoly.
Medicines which are contraindicated for simultaneous use with Veloz
Mechanism and risk factors
Therapeutic action of an atazanavir can decrease
Thanks to the anti-secretory action Veloz raises рН a stomach, reduces solubility of an atazanavir of sulfate and by that reduces its concentration in a blood plasma.
Lekastveny means, prmenyaemy with care:
Mechanism and risk factors
Level of concentration of digoxin and methyldigoxin in blood can increase.
Thanks to the anti-secretory action Veloz can increase рН a stomach that leads to the accelerated absorption of digoxin and methyldigoxin.
Level концентрац і ї an itrakonazola and a gefitiniba in blood can decrease.
Thanks to the anti-secretory function Veloz is capable to increase рН a stomach that that gefitiniba leads to inhibition of absorption of an itrakonazol.
Antacid which contain aluminum magnesium hydroxide hydroxide
Concentration of a rabeprazol can decrease at simultaneous use with antacids.
Hypersensitivity to a rabeprazol, replaced benzimidazole or to any other ingredient of drug. Simultaneous use with atazanaviry.
Experience of deliberate or accidental overdose is limited. No symptoms connected with overdose are revealed. The maximum dose did not exceed 180 mg of a rabeprazol of sodium during treatment of a syndrome of Zollingera-Ellison once a day.
Treatment. A specific antidote for Veloso the unknown. Sodium рабепразол well contacts proteins of plasma and it is not removed during dialysis. At overdose it is necessary to carry out symptomatic and supporting treatments.
To store at a temperature not above 25 °C. A period of validity - 2 years. To store in the place, unavailable to children.
According to the recipe
On 10 tablets in a strip, on 2 or 3 strips in cardboard packaging.