Ganaton

General characteristics. Structure:

Active agent — an itoprida a hydrochloride of 50 mg; auxiliary components (mg in 1 tablet): lactose — 34,975 (including surplus owing to loss in weight by production — 2,93%), starch corn — 15,0, a karmelloza — 20,0, anhydrous silicic acid — 4,0, magnesium stearate — 1,0, a gipromelloza — 4,4, a macrogoal 6000 — 0,4, titanium dioxide — 0,2, wax a Brazilian wax palm — 0,025.

Description: white round tablets, film coated, with risky on one party and an engraving of "HC 803" on another.

Pharmacological properties:

Action mechanism

Itoprida a hydrochloride increases motility of a GIT due to antagonism of D2 - dopamine receptors and inhibition of acetylcholinesterase. Itoprid activates release of acetylcholine and suppresses its destruction.

Pharmacodynamics. Itoprida a hydrochloride gives also antiemetic effect due to interaction with D2 receptors, located in a trigger zone. Itoprid caused dozozavisimy suppression of the vomiting caused by Apomorphinum.

Itoprida a hydrochloride activates propulsive motility of a stomach due to antagonism of D2 receptors and dozozavisimy inhibition of activity of acetylcholinesterase.

Itoprida a hydrochloride has specific effect on an upper part of a GIT, accelerates transit on a stomach and improves its emptying.

Itoprida a hydrochloride does not influence serumal levels of gastrin.

Pharmacokinetics. Absorption

Itoprida a hydrochloride is quickly and almost completely soaked up in a GIT. Relative bioavailability makes it 60% that is connected with metabolism at the first passing through a liver. Food does not exert impact on bioavailability. The maximum concentration in plasma (Smakh) of 0,28 mkg/ml is reached in 0,5-0,75 h after reception of 50 mg of an itoprid of a hydrochloride.

At repeated reception of an itoprid of a hydrochloride inside in a dose of 50-200 mg three times a day within 7 days the pharmacokinetics of drug and its metabolites was linear, and cumulation was minimum.

Distribution

Itoprida a hydrochloride for 96% contacts proteins of plasma, generally albumine. Linkng with an alfa1-acid glycoprotein makes less than 15% of the general binding.

Itoprid is actively distributed in fabric (volume of distribution of 6,1 l/kg) and it is found in high concentration in kidneys, a small intestine, a liver, adrenal glands and a stomach. Penetration into a head and spinal cord minimum. Itoprid gets into breast milk.

Metabolism

Itoprid is exposed to active biotransformation in a liver at the person. 3 metabolites are identified, only one of which shows small activity which has no pharmacological value (about 2-3% of that of an itoprid). Primary metabolite at the person is N-oxide which is formed as a result of oxidation of quarternary amino-N-dimethylated group.

Itoprid is metabolized under action flavin - dependent monooxygenase (FMO3). The quantity and efficiency of isoenzymes of FMO at the person can differ depending on genetic polymorphism which in rare instances leads to development of an autosomal and recessive state known under the name of a trimetilaminuriya (a syndrome of "a smell of fish"). At patients with a trimetilaminuriya the period of semi-elimination of an itoprid increases.

According to the pharmacokinetic researches in vivo, итоприд has no the inhibiting or inducing effect on CYP2C19 and CYP2E1. Therapy itopridy does not influence CYP or activity of an uridindifosfatglyukuroniziltransferaza.

Removal

Itoprid the hydrochloride and its metabolites are removed generally with urine. Renal excretion of an itoprid and its N-oxide after a single dose of drug inside in therapeutic doses at healthy people made 3,7 and 75,4% respectively. The terminal period of semi-elimination of an itoprid of a hydrochloride equals about 6 h.

Indications to use:

Itoprid a hydrochloride is applied to a symptomatic treatment of functional not ulcer dyspepsia (chronic gastritis), in particular by stoppings of abdominal distention, bystry saturation, pain or discomfort in an upper half of a stomach, anorexia, heartburn, nausea and vomiting.

Route of administration and doses:

Usually adult appoint inside on 1 tablet of Ganaton 50 mg 3 times a day to food. The recommended daily dose makes 150 mg. The specified dose can be lowered taking into account age of the patient.

Side effects:

From blood and lymphatic system: leukopenia, thrombocytopenia.

Allergic reactions: dermahemia, skin itch, rash, anaphylaxis.

Endocrine disturbances: increase in level of prolactin, gynecomastia.

From a nervous system: dizziness, headache, tremor.

From a GIT: diarrhea, a lock, an abdominal pain, the increased salivation, nausea, jaundice.

Changes of laboratory indicators: increase in activity of aspartate aminotransferase (ACT), alaninaminotranspherase (ALT), gammaglyutamiltranspeptidaza, alkaline phosphatase and level of bilirubin.

Interaction with other medicines:

Metabolic interaction is hardly possible as итоприд it is metabolized under the influence of flavin monooxygenase, but not CYP450.

At simultaneous use of warfarin, diazepam, diclofenac of sodium, a tiklopidin of a hydrochloride, nifedipine and a nikardipin of a hydrochloride of changes of linkng with proteins did not observe.

Itoprid increases motility of a stomach therefore it can influence absorption of other drugs which appoint inside. Extra care should be observed at use of drugs with a low therapeutic index, and also forms with the slowed-down release of active agent or drugs with an enterosoluble cover.

Antiulcerous means, such as Cimetidinum, ranitidine, тепренон and цетраксат, do not influence pro-kinetic action of an itoprid.

Anticholinergics can weaken effect of an itoprid.

Contraindications:

- Hypersensitivity to an itoprid or any auxiliary component of drug;
- patients with gastrointestinal bleeding, mechanical obstruction or perforation;
- children's age (up to 16 years);
- pregnancy and period of a lactation.

With care it is applied

Owing to strengthening itopridy actions of acetylcholine, it is necessary to appoint with care because of possible development of cholinergic side reactions in category of patients for whom their emergence can aggravate a current of a basic disease.

Use during pregnancy and when feeding by a breast

Ganaton is recommended to apply during pregnancy and a lactation only when there is no safer alternative, and the expected advantage outweighs possible risk.

Overdose:

Overdose cases at the person are not described. At overdose the gastric lavage and symptomatic therapy are shown.

Storage conditions:

List B. At a temperature below 25 °C, in the dry, protected from light place. Drug should be stored in the places unavailable to children. Period of validity of 5 years. Not to apply after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, coated, 50 mg.

On 7, 10 or 14 tablets in the blister from PVH/AL foil. 1, 2, 3, 4 or 5 blisters with the application instruction in a cardboard pack.