Included in the formulation
Pharmacodynamics:Strengthens the motility of the gastrointestinal tract due to antagonism with D2-dopamine receptors and inhibition of acetylcholinesterBasics. Oppression of acetylcholinesterAse activates the release of acetylcholine, suppresses its destruction. Has antiemetic effect due to interaction with D2-receptors, located in the trigger zone. Causes a dose-dependent suppression of emesis caused by apomorphine. Activates propulsive motility of the stomach due to antagonism with D2-receptors and dose-dependent inhibition of acetylcholinester activityBasics. Has a specific effect on the upper gastrointestinal tract, accelerates transit through the stomach, improves its emptying. Has no effect on serum concentrations of gastrin.
Pharmacokinetics:Quickly and well absorbed in the digestive tract. Relative bioavailability is 60%. Cmax - 0.28 μ / ml, TCmax - 0.5-0.75 hours after taking 50 mg of the drug. At repeated admission to 50-200 mg 3 times a day for 7 days pharmacokinetics is linear, cumulation is minimal.Linkage with proteins - 96% (mainly with albumin, with alpha-1-acid glycoprotein - less than 15%). It is distributed in the kidneys, small intestine, liver, adrenal gland, stomach. The volume of distribution is 6.1 l / kg. In therapeutic doses, it penetrates insignificantly into the brain and spinal cord, into breast milk. Metabolised in the liver under the action of flavin-dependent monooxygenase. Three metabolites have been identified, only one of them exhibits insignificant activity (2-3% of the totalopride activity) that does not have pharmacologicalth value. It is excreted by the kidneys. Half-life - 6 h, in patients with trimethylaminurieth half-life increases.
Indications:Symptomatic treatment of functional non-ulcer dyspepsia (chronic gastritis): flatulence, gastralgia, a feeling of discomfort in the epigastric region, anorexia, heartburn, nausea, vomiting.
XI.K20-K31.K29 Gastritis and duodenitis
XI.K20-K31.K30 Dyspepsia
XVIII.R10-R19.R10.1 Pain localized in the upper abdomen
XVIII.R10-R19.R11 Nausea and vomiting
XVIII.R10-R19.R12 Heartburn
XVIII.R10-R19.R14 Meteorism and related conditions
XVIII.R50-R69.R63.0 Anorexia
Contraindications:Hypersensitivitygastrointestinalbleeding, mechanical obstruction and perforation of the gastrointestinal tract, children's age (under 16 years), pregnancy, lactation.
Carefully:Caution should be applied itopride in patients for whom the appearance of cholinergic adverse reactions (associated with increased effect of acetylcholine under the influence of aspoid) can aggravate the course of the underlying disease. Due to the presence of lactose in the formulation, itopride use with caution in congenital deficiency of lactase, lactose intolerance, glucose-galactosemalabsorption and in geriatrics in elderly patients with reduced liver and kidney function.
Pregnancy and lactation:Contraindicated in pregnancy and lactation (breastfeeding).
Dosing and Administration:Inside, before meals, 50 mg 3 times a day, daily dose - 150 mg.
In elderly patients, the dose is reduced.
Side effects:From the hematopoiesis: leukopenia, thrombocytopenia.
Allergic reactions: urticaria, anaphylactic shock.
From the endocrine system: gynecomastia, hyperprolactinemia.
From the digestive system: increased salivation, nausea, diarrhea, constipation, jaundice.
From the nervous system: headache, dizziness, tremor.
Laboratory indicators: increased activity of hepatic transaminases, gamma-glutamyl transferase, alkaline phosphatase, hyperbilirubinemia.
Overdose:Treatment: gastric lavage, symptomatic therapy.
Interaction:Accelerates the absorption of other drugs.
Prokinetic effect of the drug does not change under the influence of antiulcer drugs (cimetidine, ranitidine, tetrenone, cetraxate).
Cholinergic drugs weaken the action of the drug.
Special instructions:Dopamine receptor antagonist, substituted benzamide. A new, poorly understood means.