Composition, form of production and packaging
The tablets coated with a film (white film) are white, round, with a risk on one side and engraving "HC 803" on the other.
1 tab.
Itopride hydrochloride 50 mg
Auxiliary substances: lactose - 34.975 mg (including excess due to loss in mass during production - 2.93%), corn starch - 15 mg, carmellose - 20 mg, silicic acid anhydrous - 4 mg, magnesium stearate - 1 mg, hypromellose - 4.4 mg, macrogol 6000 - 0.4 mg, titanium dioxide - 0.2 mg, carnauba wax - 0.025 mg.
10 pieces. - blisters (1) - packs of cardboard.
10 pieces. - blisters (4) - packs of cardboard.
14 pcs. - blisters (5) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2015.
PHARMACHOLOGIC EFFECT
A drug that increases the motility of the gastrointestinal tract. Stimulator of the release of acetylcholine.
Itopride hydrochloride activates propulsive motility of the stomach due to antagonism with dopamine D 2 receptors and a dose-dependent inhibition of acetylcholinesterase activity. Itopride activates the release of acetylcholine and suppresses its destruction.
The drug also has antiemetic effect due to interaction with D 2 -receptors located in the trigger zone. Itopride caused a dose-dependent suppression of emesis caused by apomorphine.
Itopride hydrochloride has a specific effect on the upper gastrointestinal tract, accelerates transit through the stomach and improves its emptying.
Itopride hydrochloride does not affect serum levels of gastrin.
PHARMACOKINETICS
Suction
Ittopride hydrochloride is quickly and almost completely absorbed from the digestive tract. Its relative bioavailability is 60%, which is associated with metabolism during the first passage through the liver. Food does not affect bioavailability.
After administration of 50 mg of tautopride hydrochloride inside C max is achieved in 0.5-0.75 h and is 0.28 Ојg / ml. At repeated administration of the drug at a dose of 50-200 mg 3 times / day for 7 days, the pharmacokinetics of the drug and its metabolites was linear, and the cumulation was minimal.
Distribution
Binding to plasma proteins (mainly with albumin) is 96%. Binding with? 1- acid glycoprotein is less than 15% of total binding.
It is actively distributed in tissues (V d 6.1 l / kg) and is found in high concentrations in the kidneys, small intestine, liver, adrenal gland and stomach. Penetrates through the BBB in minimal amounts. Excreted in breast milk.
Metabolism
Itopride is subject to active biotransformation in the liver. Three metabolites have been identified, only one of which exhibits little activity, which has no pharmacological significance (about 2-3% of that of taredrop). The primary metabolite is the N-oxide, which is formed as a result of oxidation of the quaternary amino-N-dimethyl group.
Itopride is metabolized by flavin-dependent monooxygenase (FMO3). The amount and effectiveness of FMO isoenzymes in humans may differ depending on genetic polymorphism, which in rare cases leads to the development of an autosomal recessive state known as trimethylaminuria ("fish smell" syndrome). In patients with trimethylaminuria, T2 / 2 of aspenopida increases.
According to pharmacokinetic studies in vivo, taperpride does not have an inhibitory or inducing effect on CYP2C19 and CYP2E1. The therapy with asperiod does not affect CYP or the activity of uridine diphosphate glucuronisyl transferase.
Excretion
Itopride hydrochloride and its metabolites are excreted mainly with urine. Renal excretion of tautopride and its N-oxide after a single oral intake of therapeutic doses in healthy people was 3.7 and 75.4%, respectively.
The final T 1/2 of tenthpride hydrochloride is about 6 hours.
INDICATIONS
Treatment of gastrointestinal symptoms associated with delayed gastric motility and functional non-ulcer dyspepsia (chronic gastritis), such as:
- bloating;
- a feeling of overflow in the stomach after eating;
pain or discomfort in the epigastric region;
anorexia;
- Heartburn;
- nausea;
- vomiting.
DOSING MODE
Adults prescribe inside 50 mg (1 tab.) 3 times / day before meals. The recommended daily dose is 150 mg. The specified dose can be reduced taking into account the age and symptoms of the patient.
In clinical studies, the duration of treatment with the drug Ganaton was up to 8 weeks.
SIDE EFFECT
On the part of the hematopoiesis system: leukopenia, thrombocytopenia.
Allergic reactions: skin hyperemia, skin itching, rash, anaphylaxis.
On the part of the endocrine system: increased prolactin levels, gynecomastia.
From the side of the central nervous system: dizziness, headache, tremor.
On the part of the digestive system: diarrhea, constipation, abdominal pain, increased salivation, nausea, jaundice.
Changes in laboratory indicators: increased activity of AST and ALT, GGT, APF and bilirubin level.
CONTRAINDICATIONS
- gastrointestinal bleeding, mechanical obstruction or perforation of the gastrointestinal tract;
- Pregnancy;
- the period of lactation (breastfeeding);
- Children's age till 16 years;
- Hypersensitivity to taeopride or any auxiliary component of the drug.
Carefully
As a result of the effects of acetylcholine, thiotyprid, should be administered with caution because of the possible development of cholinergic adverse reactions in the category of patients for whom their appearance may aggravate the course of the underlying disease.
Itopride should be administered with caution to elderly patients due to the frequent decrease in liver and kidney function, the presence of concomitant diseases or other treatment.
PREGNANCY AND LACTATION
There is insufficient data on the use of ticopride hydrochloride in pregnancy. Use in pregnancy is possible only if there is no alternative therapy, and the potential benefit to the mother exceeds the potential risk to the fetus.
There is a potential risk of developing adverse reactions in the infant, and there are also data on the isolation of tautopride with milk in rats. If you need to take during lactation, breastfeeding should be discontinued.
APPLICATION FOR CHILDREN
Contraindication: children under 16 years.
APPLICATION IN ELDERLY PATIENTS
Itopride should be administered with caution to elderly patients due to the frequent decrease in liver and kidney function, the presence of concomitant diseases or other treatment.
SPECIAL INSTRUCTIONS
Itopride enhances the action of acetylcholine and can cause cholinergic side reactions.
OVERDOSE
Cases of overdose in humans are not described.
In case of an overdose, gastric lavage and symptomatic therapy are indicated.
DRUG INTERACTION
Metabolic interaction is hardly possible; Itopod is metabolized by the action of flavin monooxygenase, rather than the isoenzymes of the cytochrome P450 system.
With the simultaneous application of Ganaton with warfarin, diazepam, diclofenac sodium, ticlopidine hydrochloride, nifedipine and nicardipine hydrochloride, there was no change in the binding of tocopride to proteins.
Itoprids strengthens the motility of the stomach, so it can affect the absorption of other concomitantly used drugs. Particular care should be taken when using drugs with a low therapeutic index, as well as forms with delayed release of the active substance or preparations with an enteric coating.
Anti-ulcer agents such as cimetidine, ranitidine, terrenone and cetraxate do not affect the prokinetic effect of taupride.
Anticholinergic drugs can weaken the effect of ittopride.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 5 years.
