Ganaton pills 50mg, 40pcs

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 action

Pharmacodynamics

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

Itopridee hydrochloride also has an antiemetic effect due to interaction with D2-receptors located in the trigger zone. Itopridee causes 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 from 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.

After taking 50 mg of Itopridee hydrochloride orally, Cmax is reached in 0.5-0.75 hours and is 0.28 mcg / ml. With repeated use of the drug at a dose of 50-200 mg 3 times / day for 7 days, the pharmacokinetics of the drug and its metabolites were linear, and the accumulation was minimal.

Distribution. It binds to plasma proteins (mainly albumin) by 96%. Binding to the α1-acid glycoprotein is less than 15% of the total binding.

It is actively distributed in tissues (Vd is 6.1 l/kg) and is found in high concentrations in the kidneys, small intestine, liver, adrenal glands and stomach. Penetrates the brain and spinal cord in minimal amounts. Penetrates into breast milk.

Metabolism. Itopride undergoes active biotransformation in the 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 is N-oxide, which is formed by oxidation of the quaternary amino-N-dimethyl group.

Itopridee is metabolized by flavin-dependent monooxygenase (FMO3). The number and effectiveness of FMOZ 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 T1/2 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.

Output. 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 T1 / 2 of Itopridee hydrochloride is about 6 hours.

Indications

• Bloating.
• Feelings of rapid satiation.
• Pain or discomfort in the upper abdomen.
• Anorexia.
• Heartburn.
• Nausea.
• Vomiting.

Use during pregnancy and lactation

The use of Ganaton during pregnancy and lactation is possible only in cases where there is no safer alternative, and the expected benefit to the mother outweighs the possible risk to the fetus or child.

Contraindications

• hypersensitivity to Itopride or any auxiliary component of the drug;
• gastrointestinal bleeding, mechanical obstruction or perforation of the gastrointestinal tract;
• pregnancy;
• lactation;
• children under 16 years of age.

With caution:  the drug should be used in patients for whom the occurrence of cholinergic side effects (associated with an increase in the action of acetylcholine under the influence of Itopridee) may worsen the course of the underlying disease.

Side effects

From the hematopoietic system:  leukopenia, thrombocytopenia.

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

From the endocrine system:  increased prolactin levels, gynecomastia.

From the central nervous system:  dizziness, headache, tremor.

From the digestive system:  diarrhea, constipation, abdominal pain, increased salivation, nausea, jaundice.

Changes in laboratory parameters:  increased activity of AST and ALT, GGT, alkaline phosphatase and bilirubin levels.

Interaction

Metabolic interaction is unlikely, since Itopridee is metabolized by flavin monooxygenase, and not by cytochrome P450 isoenzymes.

When Ganaton was co-administered with warfarin, diazepam, diclofenac sodium, ticlopidine hydrochloride, nifedipine, and nicardipine hydrochloride, no changes in Itopridee protein binding were observed.

Itopridee increases gastric motility, so it can affect the absorption of other drugs used simultaneously 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 preparations with an enteric 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

Adults: prescribed orally 50 mg (1 tablet) 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.

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.

Form of production

Pills.

Storage conditions

Store in a dry place, protected from light, at a temperature not exceeding 25 °C

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, Flatulence, Gastrointestinal motility disorders, Gastritis