Итопра®

General characteristics. Structure:

Active ingredient: 50 mg of an itoprid of a hydrochloride.

Excipients: lactoses monohydrate, starch corn, hypro rod, karmelloza of sodium, magnesium stearate.

Cover: опадрай OY-S-7223, hypro rod, gipromelloza, titanium dioxide, macrogoal-400.

Pharmacological properties:

Pharmacodynamics. Itoprida a hydrochloride increases motility of digestive tract due to antagonism with D2 - dopamine receptors and acetylcholinesterase inhibition. Itoprida a hydrochloride activates release of acetylcholine, suppresses its destruction. Itoprida a hydrochloride has antiemetic effect due to interaction with D2 - the receptors which are in a trigger zone. Causes dozozavisimy suppression of the vomiting caused by Apomorphinum.

Itoprida a hydrochloride activates propulsive motility of a stomach due to antagonism with D2 - receptors and dozozavisimy inhibition of activity of acetylcholinesterase. Itoprida a hydrochloride has specific effect on upper parts of digestive tract, accelerates transit on a stomach, improves its emptying. Does not exert impact on serumal concentration of gastrin.

Pharmacokinetics. Absorption. Itoprida a hydrochloride is quickly and well soaked up in digestive tract. Relative bioavailability - 60%. The maximum concentration in a blood plasma (Cmax) - 0,28 ¼¬/ml. The period of achievement of the maximum concentration in a blood plasma (TCmax) - 0,5-0,75 hours after reception of 50 mg of drug. At repeated reception on 50-200 mg 3 times a day within 7 days the pharmacokinetics has linear character, cumulation of drug is minimum.

Communication with proteins makes 96% (generally with albumine); with alfa1 - an acid glycoprotein - less than 15%.

Distribution. Itoprida a hydrochloride is distributed in kidneys, a small intestine, a liver, adrenal glands, a stomach. The volume of distribution (Vd) - 6,1 l/kg.

In therapeutic doses of an itoprid the hydrochloride slightly gets into a head and spinal cord, and also into breast milk.

Metabolism and removal. Drug is metabolized in a liver under action flavin - dependent monooxygenase. 3 metabolites are identified, only one of them shows insignificant activity (2 - 3% of activity of an itoprid of a hydrochloride) that has no pharmacological value.

Itoprid the hydrochloride and its metabolites are removed generally by kidneys. The elimination half-life (T1/2) - makes 6 hours, at patients from trimetilaminuriy T1/2 increases.

Indications to use:

Symptomatic treatment of functional not ulcer dyspepsia (chronic gastritis), in particular - stopping of abdominal distention (meteorism), pains or sensations of discomfort in epigastric area (gastralgia), anorexias, heartburn, nausea, vomitings, feelings of bystry saturation.

Route of administration and doses:

Inside, to food, on 50 mg 3 times a day.

The recommended daily dose makes 150 mg. The specified dose can be lowered taking into account age of the patient.

Features of use:

With care it is necessary to use drug of Igopr at patients for whom emergence of the cholinergic side reactions (connected with strengthening of action of acetylcholine under the influence of drug), can aggravate a current of a basic disease.

The instruction, if necessary, features of effect of medicine at the first reception or at its cancellation. At drug withdrawal of Itopr of signs of emergence of a withdrawal it is not described.

Use at pregnancy and in the period of a lactation. Itopra is contraindicated at pregnancy and in the period of a lactation (breastfeeding).

Data on possible influence of medicine for a medical use on ability to manage vehicles, mechanisms. Action of components of drug does not lead to disturbance of psychomotor reactions, however in connection with possible side effects (dizziness, a tremor) it is impossible to exclude decrease in concentration of attention and influence on ability of driving of motor transport and control of mechanisms.

Side effects:

From bodies of a hemopoiesis: leukopenia, thrombocytopenia.

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

From endocrine system: gynecomastia, increase in level of prolactin.

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

From a nervous system: headache, dizziness, tremor.

Laboratory indicators: increase in activity of an aspartatamipotrasferaza (ACT), alaninaminotranspherase (ALT), gammaglutamiltranspeptidaza, alkaline phosphatase, bilirubin level.

Interaction with other medicines:

Metabolic interaction is hardly possible as the itoprida a hydrochloride 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, nifedipip and nikardiiin of a hydrochloride of changes of linkng with proteins did not observe.

Itoprida a hydrochloride 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 a kishechnorastvorimy cover.

Pro-kinetic action of an itoprid of a hydrochloride does not change under the influence of antiulcerous means (циметидип, ranitidine, тепренон, цстраксат). Anticholinergic medicines weaken effect of drug.

Contraindications:

Hypersensitivity to an itoprid or any auxiliary component of drug, gastrointestinal bleedings, mechanical obstruction and perforation of bodies of digestive tract, children's age up to 16 years, pregnancy and the period of a lactation (breastfeeding).

With care: in connection with existence in composition of drug of lactose, итоприд apply with care at inborn deficit of lactase, a lactose intolerance, glyukozo-galaktozny malabsorption and in geriatrics at elderly patients with reduced function of a liver and kidneys.

Overdose:

Overdose cases at the person are not described.

Treatment: at possible overdose the gastric lavage and symptomatic therapy is shown.

Storage conditions:

In the dry, protected from light place at a temperature of nanosecond above 25 °C. To store in the place, unavailable to children. Special precautionary measures at destruction of unused medicines. Special precautionary measures at destruction of unused medicines are not required. A period of validity - 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, 50 mg. On 10 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3, 4, 5, 10 blister strip packagings on 10 tablets together with the application instruction in a cardboard pack.