Itoprid
When ATH:
A03FA
Pharmacological action.
Itoprida hydrochloride increases motoriku stomach due to antagonism D2-dopaminovykh receptors and acetylcholinesterase inhibition. Itoprid activates the release of acetylcholine and suppresses its destruction.
Itoprida hydrochloride is also anti-Emetic effect through the interaction with D2-receptors, located in the trigger zone. Itoprid caused a dose-dependent inhibition of vomiting, caused by apomorfinom.
Itoprida hydrochloride activates propul'sivnuju stomach motility due to D2-receptor antagonism and inhibition of acetylcholinesterase activity dose-depending.
Itoprida hydrochloride has a specific effect on the upper section of the GASTROINTESTINAL TRACT, speeds up transit through the stomach and improves its emptying.
Itoprida hydrochloride does not affect serum levels of gastrin.
Itoprida hydrochloride is rapidly and almost completely absorbed in the digestive tract. Relative bioavailability is 60%, that has to do with the metabolism of the first passage through the liver. Food does not affect the bioavailability. The maximum concentration in plasma is 0,28 µg/ml achieved through 0.5-0.75 hours after admission 50 mg itoprida hydrochloride.
The readmission itoprida hydrochloride inside the dose of 50-200 mg 3 twice a day for 7 days of pharmacokinetics of the drug and its metabolites was linear, While cumulation proved to be minimal.
Itoprida hydrochloride on 96% bound to plasma proteins, mostly to albumin. Alfa1-binding acid glikoproteinom is less than 15% General binding.
Itoprid actively distributed in tissues (volume of distribution 6,1 l / kg) and detected in high concentrations in the kidneys, small intestine, liver, the adrenal glands and the stomach. Penetration into the brain and spinal cord minimum. Penetrates into breast milk Itoprid.
Itoprid undergoes active biotransformation in the liver in humans. Identified 3 metabolite, only one of which shows a small activity, which has no pharmacological value (approximately 2-3% of such itoprida). The primary metabolite in humans is N-oxide, which is formed by the oxidation of Quaternary amino-N-dimetil′noj group.
Itoprid is metabolized under the influence of flavinzavisimoj monooksigenazy. Number and effectiveness of isoenzymes in human monooksigenazy flavinzavisimoj may differ depending on genetic polymorphism, that in rare cases leads to the development of autosomnorecessivnogo State, known as trimetilaminurii ("fish odor syndrome"). In patients with trimetilaminuriej period polujeliminacii itoprida increases.
According to pharmacokinetic studies in vivo, itoprid has no inhibitory or inducing acts on CYP 2C19 and CYP 2E1. Itopridom therapy does not affect CYP activity or uridindifosfatglûkuroniziltransferazy.
Itoprida hydrochloride and its metabolites are excreted mainly with urine. Itoprida renal excretion and its N-oxide after a single intake of therapeutic doses in healthy people was 3,7 and 75,4% respectively.
The Terminal half-life of itoprida hydrochloride is about 6 no.
Testimony.
Itoprida hydrochloride used for symptomatic treatment of functional non-ulcer dyspepsia (chronic gastritis), in particular, edema abdominal distention, Quick saturation, pain or discomfort in the upper abdomen, anoreksii, Heartburn, nausea and vomiting.
Dosage regimen.
Usually adults appoint inwards to 1 Tablet itoprida hydrochloride 50 mg 3 times a day before meals. The recommended daily dose is 150 mg. The specified dose can be reduced, taking into account the age of the patient.
Contraindications.
Hypersensitivity to itopridu or to any component of the drug support; patients with gastrointestinal bleeding, mechanical obstruction or perforation; Children under the age of 16 years; Pregnancy and lactation.
Side effects.
From the blood and lymphatic system: leukopenia, thrombocytopenia.
Allergic reactions: dermahemia, itching, rash, anaphylaxis.
Endocrine disorders: elevated prolactin levels, gynecomastia.
From the nervous system: dizziness, headache, tremor.
On the part of the digestive tract: diarrhea, constipation, abdominal pain, increased salivation, nausea, jaundice.
Changes in laboratory parameters: increased activity of Asat, alanine aminotransferase Alat, gamma-glutamiltranspeptidaza, ALP and bilirubin levels.
Cautions.
Due to increased itopridom action of acetylcholine, It should be administered with caution due to possible development of cholinergic side effects in patients ' category, for which their appearance can aggravate the course of the basic disease.
Use during pregnancy and breastfeeding is recommended only in cases, When there is a safer alternative, and the expected benefits outweigh the possible risks.
Drug Interactions.
Metabolic interaction is unlikely, because itoprid is metabolized under the influence of flavinovoj monooksigenazy, rather than P450.
Together with the use of warfarin, diazepama, diclofenac sodium, tiklopidina hydrochloride, nifedipine and nikardipina hydrochloride changes of bonding with the squirrels are not observed.
Itoprid strengthens motoriku stomach, Therefore, it can affect the absorption of other drugs, who appointed Interior. Special caution should be exercised when applying the preparations with a low therapeutic index, as well as the forms with a slow release of the active substance or drugs with enteric-soluble shell.
Peptic ulcer remedies, such as cimetidine, ranitidine, teprenon and cetraksat, do not affect prokinetičeskoe activity itoprida.
Antiholinergicakie funds can reduce the effect itoprida.
Overdose.
Cases of overdose have not been described in humans. Overdose showing gastric lavage and symptomatic therapy.
