Itopride hydrochloride
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Pharmacological properties
Itopride hydrochloride activates gastrointestinal propulsive motility due to antagonism with dopamine d2 receptors and the inhibitory activity of acetylcholinesterase. Itopride hydrochloride activates the release of acetylcholine and inhibits its decomposition.
Itopride hydrochloride also has an antiemetic effect due to interaction with D2-receptors localized in the chemoreceptor trigger zone, which is demonstrated by dose-dependent inhibition of apomorphine-induced vomiting in animals.
The action of itopride hydrochloride is highly specific relative to the upper gastrointestinal tract.
Itopride hydrochloride does not affect the level of gastrin in the blood plasma.
Pharmacokinetics
Absorption. Ganaton is rapidly and almost completely absorbed in the digestive tract. Its relative bioavailability is 60%, which is associated with the effect of the first passage through the liver. Food does not affect bioavailability. After applying 50 mg of itopride hydrochloride Cmax achieved after 0.5-0.75 h and is 0.28 μg / ml. With further use of the drug in doses of 50 to 200 mg 3 times a day for 7 days, the pharmacokinetics of itopride hydrochloride and its metabolites were linear with minimal cumulation.
Distribution. Approximately 96% of itopride hydrochloride binds to blood plasma proteins (mainly albumin). Linking with α1-acid glycoprotein is less than 15%.
Metabolism. Itopride hydrochloride is actively biotransformed in the liver. 3 metabolites have been identified, only 1 of which shows insignificant activity, which has no pharmacological significance (approximately 2-3% of itopride hydrochloride). The primary metabolite is the N-oxide resulting from the oxidation of the quaternary amino-N-dimethyl group.
Itopride hydrochloride is metabolized by flavin-dependent monooxygenase (FMO). The amount and effectiveness of FMO isoenzymes in humans may vary depending on genetic polymorphism, which sometimes leads to the development of an autosomal recessive condition known as trimethylaminuria (fish smell syndrome). In patients with trimethylaminuria T½ increases.
According to in vivo pharmacokinetic studies, itopride hydrochloride has no inhibitory or inducing effect on CYP 2C19 and CYP 2E1. The use of itopride hydrochloride does not affect the content of CYP or the activity of uridine diphosphate glucuronisyl transferase.
Itopride hydrochloride and its metabolites are excreted mainly in urine. The renal excretion of itopride hydrochloride and its N-oxide was 3.7 and 75.4%, respectively, after a single dose of the drug in healthy volunteers at a therapeutic dose.
Terminal T½ itopride hydrochloride was about 6 hours
Indications
Relieving the gastrointestinal symptoms of functional non-ulcer dyspepsia (chronic gastritis), namely: bloating; a feeling of quick satiation; pain and discomfort in the upper abdomen; anorexia; heartburn; nausea; vomiting
Application
For adults, the recommended dose of ganaton is 150 mg / day (1 tablet (50 mg) 3 times a day before meals). the indicated dose can be reduced taking into account the patients age and symptoms.
Contraindications
Hypersensitivity to itopride hydrochloride or other components of the drug. conditions in which an increase in contractile activity of the gastrointestinal tract can be harmful, for example, with gastrointestinal bleeding, mechanical obstruction, or perforation.
Side effects
Adverse reactions reported in clinical trials. during clinical trials (phase i – iii), itopride hydrochloride was well tolerated and no serious adverse reactions were reported.a total of 19 cases of adverse reactions were reported, which were noted in 14 of 572 patients, which is 2.4%. most of the observed adverse reactions that were observed in more than 1 patient were: diarrhea (0.7%), headache (0.3%), abdominal pain (0.3%). deviations of laboratory parameters that were noted during clinical trials: a decrease in the level of leukocytes (leukopenia) (0.7%), an increase in prolactin level (0.3%).
Adverse reactions reported during post-marketing surveillance and clinical trials (which are ongoing) in patients receiving treatment with itoprid hydrochloride
From the blood system and lymphatic system: leukopenia, thrombocytopenia.
From the immune system: anaphylactoid reactions.
From the endocrine system: increased levels of prolactin, gynecomastia.
From the nervous system: dizziness, headache, tremor.
From the digestive system: diarrhea, constipation, abdominal pain, increased salivation, nausea.
On the part of the liver and biliary tract: jaundice.
On the part of the skin and subcutaneous tissue: rash, redness, itching.
Laboratory studies: increased levels of AcAT, AlAT, γ-glutamyltranspeptidase, alkaline phosphatase, bilirubin.
special instructions
Itopride hydrochloride enhances the action of acetylcholine and may exhibit cholinergic adverse reactions. data on long-term use are not available. Itopride hydrochloride should be prescribed with caution to elderly patients.
Use during pregnancy and lactation. Itopride hydrochloride should not be used during pregnancy. Itopride hydrochloride passes into breast milk. An appropriate decision must be made regarding discontinuation of breastfeeding or discontinuation of treatment, given the importance of therapy to the mother.
Children. The safety of itopride hydrochloride in children under 16 years of age has not been established.
The ability to influence the reaction rate when driving vehicles or working with other mechanisms. Information on the possible effect on the reaction rate is not available, but when deciding on the issue of driving or working with other mechanisms, it is necessary to take into account the possibility of dizziness.
Interactions
Metabolic interactions are not expected due to the fact that itopride hydrochloride is primarily metabolized by flavin monooxygenase and not by isoenzymes of the p450 cytochrome system.
No changes were noted regarding protein binding when used concomitantly with warfarin, diazepam, diclofenac, ticlopidine, nifedipine and nicardipine hydrochloride. Due to the fact that itopride hydrochloride enhances the motility of the stomach, it can affect the absorption of other drugs with simultaneous use. Caution should be exercised when using drugs with a low therapeutic index, sustained release dosage forms, or enteric coating.
Antiulcer drugs, such as cimetidine, ranitidine, teprenone and cetraxate, do not affect the prokinetic effect of itopride hydrochloride.
Anticholinergic drugs may decrease the effects of itopride hydrochloride.
Overdose
No cases of overdose have been reported.
Treatment. In case of an overdose, it is necessary to take the usual measures for gastric lavage and symptomatic treatment.
Storage conditions
It does not require special storage conditions.
Conditions of dispensing from pharmacies: by prescription.
PR-UA-GAN-18 (10/14)
184 Items
2020-07-30
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