Retch pills 50mg, 70pcs

Composition

of 1 tab. :

Active ingredient:

• Itopridee hydrochloride 50,00 mg;

excipients:

• lactose monohydrate 65.56 mg,
• pregelatinized starch 1.20 mg,
• croscarmellose sodium 1.20 mg,
• colloidal anhydrous silicon dioxide 0.84 mg,
• magnesium stearate 1.20 mg

Pharmacological action

Gastrointestinal Motility stimulator-acetylcholine release stimulator.

Pharmacokinetics

Suction

It is rapidly and almost completely absorbed into the gastrointestinal tract. Its relative bioavailability is 60%, which is associated with metabolism at the first passage through the liver.

The maximum plasma concentration (Cmax) of 0.28 mcg / ml, after taking 50 mg of the drug, is reached in 0.5-0.75 hours

With repeated oral use of the drug at a dose of 50-200 mg three times a day for 7 days, the pharmacokinetics are linear, the accumulation is minimal.

Distribution

It binds to 96% of plasma proteins, mainly albumin. Binding to alpha-1-acid glycoprotein is less than 15%.

It is actively distributed in tissues (volume of distribution 6.1 l / kg) and is found in high concentrations in the kidneys, small intestine, liver, adrenal glands and stomach. In therapeutic doses, it slightly penetrates into the brain and spinal cord, into breast milk.

Metabolism

It is metabolized in the liver. 3 metabolites were identified, one of which exhibits insignificant activity that has no pharmacological significance (approximately 2-3% of that of Itopridee). The primary metabolite in humans is N-oxide, which is formed as a result of oxidation of the quaternary amino-N-dimethyl group.

It is metabolized by flavin-dependent monooxygenase (FMO3). The number and effectiveness of human isoenzymes can vary depending on the genetic polymorphism that in rare cases leads to the development of an autosomal recessive condition known as trimethylaminuria (fish smell syndrome).

In patients with trimethylaminuria, the half-elimination period of the drug increases.

The drug has no inhibitory or inducing effect on CYP2C19 and CYP2E1. The use of Itopridee does not affect the activity of uridine diphosphate glucuronisyltransferase.

Deduction

Itopridee and its metabolites are excreted by the kidneys. Renal excretion of Itopridee and its N-oxide after a single oral dose of the drug in therapeutic doses in healthy people was 3.7 and 75.4%, respectively.

The half-life of the drug (T 1/2) is 6 hours

. Pharmacodynamics

Increases the motility of the gastrointestinal tract (GIT) by antagonizing D2-dopamine receptors and inhibiting acetylcholinesterase. Activates the release of acetylcholine and inhibits its breakdown.

It has an antiemetic effect due to interaction with D2-receptors located in the trigger zone. Causes dose-dependent suppression of apomorphine-induced vomiting.

Activates the propulsive motility of the stomach due to D2-receptor antagonism and dose-dependent inhibition of acetylcholinesterase activity.

The effect of the drug in patients with functional dyspepsia leads to a decrease in the severity of symptoms (general assessment by the patient, postprandial heaviness in the abdomen, early satiety).

The use of Itopridee in patients with diabetic gastroparesis accelerated the evacuation of liquid and solid food from the stomach.

In patients with gastroesophageal reflux disease (GERD), Itopridee reduces the amount of transient relaxation of the lower esophageal sphincter and reduces the duration of time with high esophageal acidity (pH

It has a specific effect on the smooth muscles of the gastrointestinal tract, accelerates Tranzit through the stomach and improves its emptying. It does not affect serum gastrin concentrations.

Indications

It is used to treat gastrointestinal symptoms associated with impaired gastric motility or delayed emptying, such as bloating, rapid satiety, a feeling of fullness in the stomach after eating, pain or discomfort in the epigastric region, decreased appetite, heartburn, nausea and vomiting; functional (non-ulcerative) dyspepsia or chronic gastritis.

Use during pregnancy and lactation

Pregnancy

There are insufficient data on the use of Itopridee hydrochloride in pregnant women. Use during pregnancy is possible only when there is no alternative therapy, and the potential benefit to the mother exceeds the potential risk to the fetus.

Breast-feeding period

There is a potential risk of developing adverse reactions in an infant, and there are also data on the excretion of Itopridee in milk in rats. If it is necessary to take it during lactation, breastfeeding should be discontinued.

Contraindications

Hypersensitivity to Itopride or any auxiliary component of the drug; patients with gastrointestinal bleeding, mechanical obstruction or perforation; children (up to 16 years); pregnancy and lactation; lactase deficiency, lactose intolerance, glucose-galactose malabsorption.

Caution should be used in patients for whom the development of cholinergic side effects (associated with increased action of acetylcholine during drug therapy) may worsen the course of the underlying disease; patients with impaired liver and kidney function; elderly patients.

Side effects

World Health Organization (WHO) classification of adverse reactions by frequency: very common (≥ 1/10), common (≥ 1/100 and higher).

Disorders of the blood and lymphatic system: infrequently-leukopenia, frequency unknown-thrombocytopenia.

Immune system disorders: rarely-skin hyperemia, pruritus, rash, frequency unknown – anaphylactoid reactions.

Endocrine system disorders: infrequently-hyperprolactinemia, frequency unknown-gynecomastia.

Nervous system disorders: infrequently – dizziness, headache, sleep disturbance, irritability, frequency unknown-tremor.

Gastrointestinal disorders: infrequently – diarrhea, constipation, abdominal pain, increased salivation, frequency unknown-nausea, jaundice.

Musculoskeletal and connective tissue disorders: Infrequently-chest or back pain.

Effects on the results of laboratory and instrumental studies: infrequently-increased blood creatinine and urea nitrogen (BUN), frequency unknown – increased activity of aspartate aminotransferase (ACT), alanine aminotransferase (ALT), gammaglutamyltranspeptidase, alkaline phosphatase and bilirubin.

Other: infrequently-fatigue.

Interaction

No interaction was found when Itopridee was co-administered with warfarin, diazepam, diclofenac, ticlopidine, nifedipine, and nicardipine.

Metabolic interaction at the level of isoenzymes of the CYP450 system is not expected, since Itopridee is mainly metabolized by flavin monooxygenase.

Itopridee enhances gastric motility, which may affect the absorption of drugs when used together inside. Special care should be taken when taking drugs with a narrow therapeutic index, drugs with a prolonged release of the Active ingredient or drugs with an enteric coating.

Anti-ulcer drugs such as cimetidine, ranitidine, teprenone and cetraxate do not affect the prokinetic efficacy of Itopridee.

M-holinoblockers reduce the effectiveness of Itopridee.

The cholinergic effect of Itopridee may increase with the simultaneous use of M-cholinomimetics, as well as cholinesterase inhibitors.

How to take, course of use and dosage

Usually adults are prescribed inside 1 tablet of Retch 50 mg 3 times a day before meals.

The recommended daily dose is 3 tablets (150 mg).

The indicated dose may be reduced based on the patient’s age and symptoms.

If the drug was not taken on time, then in the future it should be taken at regular intervals. It is not recommended to take a double dose to compensate for the missed one.

In clinical trials, the duration of treatment with Itopridee was up to 8 weeks.

Overdose

Cases of overdose in humans are not described.

In case of overdose, gastric lavage and symptomatic therapy are indicated.

Special instructions

Itopridee enhances the action of acetylcholine and may cause cholinergic side effects.

Patients with impaired liver or kidney function should be carefully monitored by a doctor, and if necessary, the dose of the drug should be reduced or therapy with the drug should be discontinued.

If symptoms of galactorrhea and gynecomastia occur, treatment should be interrupted or completely discontinued.

Influence on the ability to drive motor vehicles and manage mechanisms

Studies on the effect of Itopridee on the ability to drive a car and mechanisms have not been conducted.

However, during treatment with the drug, care should be taken when performing potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions (driving vehicles, working with moving mechanisms, working as a dispatcher and operator), since the use of the drug can cause dizziness.

Active ingredient

Itopride

Conditions of release from pharmacies

By prescription

Dosage form

Tablets