Ganaton pills 50mg, 70pcs

Composition

1 tablet contains:

Active ingredient:

Itopridee hydrochloride – 50 mg;

Auxiliary substances:

lactose – 34,975 mg (including excess due to mass loss in the production of 2.93%),

corn starch is 15 mg

carmellose 20 mg,

anhydrous silicic acid – 4 mg,

magnesium stearate – 1 mg,

hypromellose – 4.4 mg,

macrogol 6000 – 0.4 mg,

titanium dioxide – 0.2 mg,

Carnauba wax – 0,025 mg.

Pharmacological properties

Pharmacotherapeutic group – the stimulator of motility of the gastrointestinal tract – acetylcholine release stimulator.

The ATX code is 03FA.

Pharmacological properties

Mechanism of action

Itopridee hydrochloride enhances gastrointestinal motility by antagonizing D2-dopamine receptors and inhibiting acetylcholinesterase. Itopridee activates the release of acetylcholine and inhibits its breakdown.

Pharmacodynamics

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

Itopridee hydrochloride activates propulsive gastric motility by antagonizing D2 receptors and dose-dependent inhibition of acetylcholinesterase activity.

Itopridee hydrochloride has a specific effect on the upper gastrointestinal tract, accelerates Tranzit through the stomach and improves its emptying.

Itopridee hydrochloride does not affect serum gastrin levels.

Pharmacokinetics

Suction

Itopridee hydrochloride is rapidly and almost completely absorbed in the gastrointestinal tract. Its relative bioavailability is 60%, which is associated with metabolism at the first passage through the liver. Food has no effect on bioavailability. The maximum plasma concentration (Cmax) of 0.28 mcg / ml is reached 0.5-0.75 hours after taking 50 mg of Itopridee hydrochloride.

With repeated oral use of Itopridee hydrochloride at a dose of 50-200 mg three times a day for 7 days, the pharmacokinetics of the drug and its metabolites were linear, and the accumulation was minimal.

Distribution

Itopridee hydrochloride is 96% bound to plasma proteins, mainly albumin. Binding to alpha-1-acid glycoprotein is less than 15% of the total binding.

Itopridee is actively distributed in the tissue (volume of distribution 6.1 l/kg) and is found in high concentrations in the kidneys, small intestine, liver, adrenal glands and stomach. Penetration into the brain and spinal cord is minimal. Itopride passes into breast milk.

Metabolism

Itopride undergoes active biotransformation in the human liver. 3 metabolites were identified, only one of which shows a small 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.

Itopridee is metabolized by flavin-dependent monooxygenase (FMO3). The number and effectiveness of FMO isoenzymes in humans may differ 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 Itopridee increases.

According to in vivo pharmacokinetic studies, Itopridee has no inhibitory or inducing effect on CYP2C19 and CYP2E1. Itopride therapy does not affect CYP or uridine diphosphate glucuronisyltransferase activity.

Deduction

Itopridee hydrochloride and its metabolites are mainly excreted in the urine. 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 terminal half-elimination period of Itopridee hydrochloride is about 6 hours.

Indications

Itopridee hydrochloride is used for the symptomatic treatment of functional non-ulcer dyspepsia (chronic gastritis), in particular relief of bloating, rapid satiety, pain or discomfort in the upper abdomen, anorexia, heartburn, nausea and vomiting.

Use during pregnancy and lactation

Use Ganaton during pregnancy and lactation is recommended only in cases where there is no safer alternative, and the expected benefit outweighs the possible risk.

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.

Apply with caution

Due to the increased effect of acetylcholine by Itopride, it should be prescribed with caution due to the possible development of cholinergic side effects in patients for whom their occurrence may worsen the course of the underlying disease.

Side effects

Blood and lymphatic system disorders:  leukopenia, thrombocytopenia.

Allergic reactions:  hyperemia of the skin, pruritus, rash, anaphylaxis.

Endocrine disorders:  increased prolactin levels, gynecomastia.

Nervous system disorders:  dizziness, headache, tremor.

From the gastrointestinal tract:  diarrhea, constipation, abdominal pain, increased salivation, nausea, jaundice.

Changes in laboratory parameters:  increased activity of aspartate aminotransferase (ACT), alanine aminotransferase (ALT), gammaglutamyltranspeptidase, alkaline phosphatase and bilirubin levels.

Interaction

A metabolic interaction is unlikely, since Itopridee is metabolized by flavin monooxygenase, and not by CYP450.

No protein binding changes were observed when warfarin, diazepam, diclofenac sodium, ticlopidine hydrochloride, nifedipine, and nicardipine hydrochloride were co-administered.

Itopridee increases the motility of the stomach, so it can affect the absorption of other drugs that are prescribed inside. Special care should be taken when using drugs with a low therapeutic index, as well as forms with a delayed release of the Active ingredient or drugs with an enteric-soluble coating.

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

Anticholinergic agents may weaken the effect of Itopridee.

How to take, course of use and dosage

Usually adults are prescribed inside 1 tablet of Ganaton 50 mg 3 times a day before meals. The recommended daily dose is 150 mg. The indicated dose can be reduced taking into account the patient’s age.

Overdose

Cases of overdose in humans are not described. In case of overdose, gastric lavage and symptomatic therapy are indicated.

Description

Film-coated tablets are white in color, round, with a risk on one side and the inscription “HC 803” on the other.

Special instructions

Due to the increased effect of acetylcholine by Itopride, the drug should be prescribed with caution due to the possible development of cholinergic side effects in the category of patients for whom their occurrence may worsen the course of the underlying disease.

Storage conditions

List B. At temperatures below 25°C, in a dry place protected from light. The drug should be stored out of the reach of children.

Shelf life

5 years

Active ingredient

Itopride

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Description

Children as prescribed by a doctor, Adults as prescribed by a doctor, Children over 16 years of age

Indications

Heartburn, Gastritis, Flatulence, Gastrointestinal motility disorders