Universal reference book for medicines
Product name: ONTIME

Active substance: rabeprazole

Type: H + -K + -ATPase inhibitor.
Antiulcer drug
Manufacturer: Teva Pharmaceutical Industries (Israel)
Composition, form of production and packaging
The tablets covered with an enteric-insoluble coat of
pink color with a brown tinge, round, biconcave, with an inscription of black color "N" and "10" on the one hand, with a weak specific odor.

1 tab.

rabeprazole sodium 10 mg

Excipients: mannitol - 11.5 mg, low-substituted giprolose - 13.15 mg, magnesium oxide - 30 mg, giprolose - 2.75 mg, magnesium stearate - 0.6 mg;
shell septil of LP-761 white (hypromellose 2910 15sR (E464) - 2.53 mg, microcrystalline cellulose - 0.55 mg, stearic acid - 0.96 mg, titanium dioxide (E171) - 0.96 mg); enteric membrane (hypromellose phthalate (HP-55) - 12.7 mg, triethyl citrate - 1.3 mg); Opaque shell II 31F24127 pink (lactose monohydrate 0.36 mg, hypromellose 2910 15 sp (E464) 0.28 mg, titanium dioxide (E171) 0.23 mg, macrogol 4000 0.1 mg, iron oxide oxide yellow 0.013 mg, iron dye oxide red, 0.017 mg).
10 pieces.
- blisters (1) - packs of cardboard.
10 pieces.
- blisters (2) - packs of cardboard.
The tablets covered with an enteric-soluble coat of yellow color, round, biconcave, with the inscription "93" and "64" on one side, with a weak specific odor.

1 tab.

rabeprazole sodium 20 mg

Excipients: mannitol - 23 mg, low-substituted giprolose - 26.3 mg, magnesium oxide - 60 mg, giprolase - 5.5 mg, magnesium stearate - 1.2 mg;
septic membrane LP-761 white (hypromellose 2910 15sR (E464) - 5.06 mg, microcrystalline cellulose 1.1 mg, stearic acid 1.92 mg, titanium dioxide (E171) 1.92 mg); enteric membrane (hypromellose phthalate (HP-55) - 19 mg, triethyl citrate - 2 mg); Opaque shell II 31F32870 yellow (lactose monohydrate 0.72 mg, hypromellose 2910 15sR (E464) 0.56 mg, titanium dioxide (E171) 0.463 mg, macrogol 4000 0.2 mg, iron dye oxide yellow 0.056 mg, iron dye oxide red - 0.001 mg, ferric oxide black oxide - 0.001 mg).
10 pieces.
- blisters (1) - packs of cardboard.
10 pieces.
- blisters (2) - packs of cardboard.
10 pieces.
- blisters (3) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2015.

PHARMACHOLOGIC EFFECT

Rabeprazole belongs to the class of antisecretory compounds, which are chemically substituted benzimidazoles.
The drug does not possess anticholinergic activity and is not a blocker of H 2 -receptors of the stomach wall, but suppresses the synthesis of hydrochloric acid by specific inhibition of the activity of the enzyme H + -K + -ATPase (acid or proton pump). This effect is dose-dependent and leads to inhibition of both basal and stimulated secretion of hydrochloric acid regardless of the stimulus. As a weak base, rabeprazole at any dose is rapidly absorbed and concentrated in the acidic environment of parietal cells and, when converted to an active sulfenamide group, sequentially interacts with the cysteines of the proton pump.
Antisecretory activity.
After oral administration of 20 mg of rabeprazole, the antisecretory effect occurs within 1 hour and reaches a maximum after 2-4 hours. The oppression of basal and food-stimulated acid secretion at 23 hours after the first dose of rabeprazole was 62 and 82%, respectively, and the duration of this action reached 48 h. The inhibitory effect of rabeprazole on the secretion of hydrochloric acid is gradually increased as a result of the daily intake of 1 tablet, the maximum level of oppression of secretion is achieved 3 days after the start of the drug. After discontinuing reception of rabeprazole secretory activity is restored after 2-3 days.
Effect on the concentration of gastrin in the blood serum.
In clinical trials, patients took 10 mg or 20 mg of rabeprazole 1 time / day with a treatment duration of up to 43 months. In the first 2-8 weeks of rabeprazole therapy, the serum gastrin concentration increased as a result of its inhibitory effect on the secretion of hydrochloric acid and returned to the baseline, usually within 1-2 weeks after discontinuation of treatment.
In special clinical studies, it has been shown that the use of rabeprazole for 36 months does not lead to histological changes in enterochromafin-like cells of biopsy specimens of the bottom and antrum of the stomach, does not affect the incidence of atrophic gastritis, intestinal metaplasia, and limits the prevalence of Helicobacter pylori infection.

Other effects.
At present, there is no evidence that rabeprazole causes systemic effects from the central nervous system, cardiovascular and respiratory systems.Rabeprazole in a daily dose of 20 mg for 2 weeks does not affect the function of the thyroid gland, the metabolism of carbohydrates, as well as the blood levels of parathyroid hormone, cortisol, estrogen, testosterone, prolactin, cholecystokinin, secretin, glucagon, follicle stimulating hormone, luteinizing hormone, renin, aldosterone and growth hormone.
PHARMACOKINETICS

Suction

Rabeprazole is cleaved under the action of hydrochloric acid, so it is used in a special enteric-soluble dosage form.
Rabeprazole is rapidly absorbed from the intestine.After taking 20 mg of C max, rabeprazole in plasma is achieved after about 3.5 hours. Changes in C max and AUC are linear in the dose range of 10 to 40 mg. Absolute bioavailability after ingestion of 20 mg (compared with the intravenous administration) is approximately 52% due to the effect of "first passage" through the liver.Bioavailability does not change with re-administration of rabeprazole. The intake of food and the time of taking the drug within a day have no effect on the absorption of rabeprazole.
Distribution

97% of rabeprazole is in plasma in a protein-related condition.

Metabolism

Rabeprazole is metabolized in the liver by the cytochrome P450 system (CYP450).
Biotransformed with the participation of the enzymes CYP2C19 and CYP3A4 with the formation of active metabolites - thioether (M1) and carboxylic acid (M6), as well as minor metabolites present in low concentrations - sulfone (M2), dimethylthioether (M4) and mercapturic acid conjugate (M5). Only dimethyl metabolite (M3) has an insignificant antisecretory activity, but it is not found in plasma.In studies in vitro, rabeprazole does not induce or inhibit the metabolism of isoenzyme CYP3A4, so any interaction of rabeprazole and cyclosporine can be ruled out.
Excretion

In healthy volunteers, T 1/2 is about 1 hour (0.7-1.5 h), the total clearance is 283 ± 98 ml / min.

After a single oral ingestion of 20 mg labeled with 14C of rabeprazole, the excretion of the active substance unchanged does not occur.
Approximately 90% of this dose is excreted in the urine mainly in the form of two metabolites: a conjugate of mercapturic acid (M5) and a carboxylic acid (M6). The rest of the drug is excreted with feces.
Pharmacokinetics in special clinical cases

After a single dose of rabeprazole at a dose of 20 mg with similar body weight and growth, no significant differences in pharmacokinetic parameters are observed with gender.

In patients at the terminal stage of renal failure requiring hemodialysis (CC less than 5 ml / min), the distribution of rabeprazole was very similar to that of healthy volunteers.
AUC and Cmax in these patients were approximately 35% lower than in healthy volunteers. On average, T 1/2 rabeprazole was 0.82 h in healthy volunteers, 0.95 h in patients during hemodialysis and 3.6 h after hemodialysis. The clearance of the drug in patients with diseases of the kidneys in need of hemodialysis was approximately 2 times higher than in healthy volunteers.
After a single dose of 20 mg rabeprazole in patients with moderate chronic liver failure, the AUC increased 2-fold and T 1/2 increased 2-3-fold as compared with healthy volunteers.
However, after taking rabeprazole 20 mg / day for 7 days, the AUC increased only 1.5 times, and C max - 1.2 times. T 1/2 in patients with hepatic insufficiency was 12.3 h compared to 2.1 h in healthy volunteers. The pharmacodynamic response (pH control in the stomach) in both groups was clinically comparable.
In elderly patients the excretion of rabeprazole is somewhat slowed down.
After 7 days after taking rabeprazole 20 mg / day in this category of patients, AUC was approximately 2 times greater, and C max - by 60% higher compared to young healthy volunteers. However, there were no signs of cumulation of rabeprazole.
In case of delayed metabolism of CYP2C19 after taking rabeprazole 20 mg / day for 7 days, the AUC increases 1.9 times, and T 1/2 - 1.6 times compared with the same parameters in extensive metabolizers, while C max increases by 40%.

INDICATIONS

- Stomach ulcer and duodenal ulcer in the phase of exacerbation;

- erosive or ulcerative gastroesophageal reflux disease (GERD);

- long-term maintenance therapy GERD;

- symptomatic treatment of GERD;

- Zollinger-Ellison syndrome;

- eradication of Helicobacter pylori in combination with antibacterial agents.

DOSING MODE

The drug is taken orally.
If the drug is taken according to the indications required to take the drug 1 time / day, you should take the pill in the morning before eating. It is established that neither the time of day nor the intake of food does not affect the activity of the drug. But the recommended time of taking the tablets contributes to better adherence to the patient's treatment regimen. Tablets should be swallowed whole, without chewing or grinding.
With gastric ulcer and duodenal ulcer in the phase of exacerbation, it is recommended to take 20 mg 1 time / day in the morning for 4-6 weeks.

In most patients with duodenal ulcer, ulcer healing occurs within 4 weeks.
It should be noted that some patients need to take Ontime for 4 weeks to heal ulcers.
In most patients with peptic ulcer disease, healing occurs within 6 weeks, but some patients may need an additional 6-week treatment with Ontimes for healing ulcers.

When erosive or ulcerative GERD is recommended to take 1 tab.
(20 mg) 1 time / day for 4-8 weeks.
For prolonged maintenance therapy GERD is recommended to take in a dose of 10 or 20 mg 1 time / day.
The duration of treatment depends on the patient's well-being.
For symptomatic treatment of GERD patients without esophagitis should be taken at a dose of 10 mg 1 time / day for 4 weeks.
If after 4 weeks of treatment the symptoms do not disappear, you should conduct an additional examination of the patient. If the symptoms of the disease are not permanent, it is recommended to take Ontime as needed in a dose of 10 mg 1 time / day.
With Zollinger-Ellison syndrome, the dose is selected individually.
The initial dose is 60 mg / day, if necessary, the daily dose can be increased to 120 mg / day and divided into 2 divided doses: 60 mg 2 times / day. The maximum single dose, as a rule, is 100 mg. Treatment should continue until the clinical effect is achieved.
Eradication of Helicobacter pylori in combination with antibacterial agents: it is recommended to perform a course of treatment of 7 days with the following combination of preparations: Ontime 20 mg 2 times / day + clarithromycin 500 mg 2 times / day and amoxicillin 1 g 2 times / day.

Patients with impaired renal or hepatic function are not required to adjust the dose of Ontime.

SIDE EFFECT

Ontimes is usually well tolerated.
Side effects, as a rule, are transient.
From the hematopoietic and lymphatic systems :? 1/10 000, but <1/1000 - leukopenia, neutropenia, thrombocytopenia.

On the part of metabolism :? 1/10 000, but <1/1000 - anorexia.

From the immune system :? 1/10 000, but <1/1000 - allergic reactions.

From the nervous system :? 1/100, but <1/10 - insomnia, headache, dizziness;
? 1/1000, but <1/100 - irritability, drowsiness; ? 1/10 000, but <1/1000 - depression.
On the part of the organs of vision :? 1/10 000, but <1/1000 - reduced visual acuity.

On the part of the respiratory system :? 1/100, but <1/10 - cough, rhinitis, pharyngitis;
? 1/1000, but <1/100 - a bronchitis, a sinusitis.
From the digestive system :? 1/100, but <1/10 - nausea, vomiting, diarrhea, increased gas formation, abdominal pain, constipation;
? 1/1000, but <1/100 - dyspepsia, belching, dryness of the oral mucosa; ? 1/10000, but <1/1000 - gastritis, stomatitis, a taste perversion.
On the part of the liver and bile ducts :? 1/1000, but <1/100 - increased activity of transaminases in the blood plasma;
? 1/10 000, but <1/1000 - hepatitis, jaundice, hepatic encephalopathy.
From the skin and subcutaneous fat :? 1/1000, but <1/100 - rash, erythema;
? 1/10 000, but <1/1000 - itching, increased sweating, bullous reactions; <1/10 000 - erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome.
From the musculoskeletal system :? 1/100, but <1/10 - nonspecific pain in the back;
? 1/1000, but <1/100 - myalgia, arthralgia, cramps in the legs.
From the urinary system :? 1/100, but <1/10 - pollakiuria, urinary retention;
? 1/1000, but <1/100 is an interstitial nephritis.
Other :? 1/100, but <1/10 - asthenia;
"1/1000, but <1/100 - chest pain, chills, fever.
CONTRAINDICATIONS

- Pregnancy;

- the period of breastfeeding;

- Hypersensitivity to rabeprazole sodium or substituted benzimidazoles, as well as to any ingredient of this drug.

With caution: a violation of the liver.

PREGNANCY AND LACTATION

Special studies on the safety of Ontime in pregnant women have not been conducted.
Therefore, the use of the drug in pregnancy is not recommended.
Experimental studies of reproductive performance in rats and rabbits showed no signs of impaired fertility or fetal development defects caused by Ontime;
However, in rats in small quantities, the drug penetrates through the placental barrier.
It is not known whether rabeprazole is excreted in breast milk.
Appropriate studies in lactating women were not conducted. However, rabeprazole is found in the milk of lactating rats, so Ontime should not be given during breastfeeding.
APPLICATION FOR FUNCTIONS OF THE LIVER

Patients with impaired renal function are not required to adjust the dose of Ontime.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

In patients with mild or moderate liver function abnormalities, there was no significant difference in the frequency of Ontimes' side effects from those of healthy and well-chosen individuals, but in spite of this, caution should be exercised when first prescribing the drug to patients with severe hepatic impairment


APPLICATION FOR CHILDREN

Ontime is not recommended for children, since there is currently no experience with its use in pediatric practice.

SPECIAL INSTRUCTIONS

Before starting therapy with Ontime, it is necessary to exclude the presence of malignant neoplasm of the stomach.
The drug may mask symptoms and delay the correct diagnosis.
Patients who are forced to take Ontime for a long time should be under constant medical supervision.

In patients with mild or moderate liver function abnormalities, there was no significant difference in the frequency of Ontimes' side effects from those of healthy and healthy individuals, but nevertheless, caution should be exercised when administering the drug for the first time to patients with severe hepatic impairment.

Use in Pediatrics

Ontime is not recommended for children, since there is currently no experience with its use in pediatric practice.

Impact on the ability to drive vehicles and manage mechanisms

Based on the characteristics of pharmacodynamics and the profile of adverse reactions of rabeprazole, it is unlikely that Ontime has an effect on the ability to drive and other mechanisms.
However, in the case of drowsiness and dizziness, these activities should be avoided.
OVERDOSE

Until now, there have been no reports of cases of deliberate overdose of Ontime.
The maximum daily dose does not exceed, as a rule, 160 mg / day. The resulting side effects are usually little expressed and do not require additional therapy.
In the event of an accidental overdose, symptomatic and supportive therapy should be given.
There is no specific antidote. The Ontem drug extensively binds to plasma proteins, so it is practically not removed during dialysis.
DRUG INTERACTION

Ontimes causes a pronounced and prolonged decrease in the production of hydrochloric acid, increasing the pH of the contents of the stomach.
Therefore, when used simultaneously with drugs, the absorption of which depends on the pH of the stomach contents, incl. ketoconazole and itraconazole, it is necessary to adjust their doses taking into account the fact that the concentration of these drugs in the blood plasma decreases.
In special studies, no interaction of Ontime with liquid antacids was found.

TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children at a temperature of no higher than 25 ° C.
Shelf life - 2 years.
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