Ganaton, 50 mg 70 pcs.

Name: Ganaton, 50 mg 70 pcs.
SKU: 214952
Availability: InStock

€23.94

EAN: 8002660008077 SKU: 214952 Categories: Bowel tone, Medicine, Stomach, intestines, liver

Description

Pharmacotherapeutic group – gastrointestinal motility stimulator – acetylcholine release stimulator.

The ATC code is A03FA.

Pharmacological properties

The mechanism of action

Itopride hydrochloride increases gastrointestinal motility by antagonizing D2-dopamine receptors and inhibiting acetylcholinesterase. Itopride activates the release of acetylcholine and inhibits its degradation.

Pharmacodynamics

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

Itopride hydrochloride activates gastric propulsive motility through antagonism of D2 receptors and dose-dependent inhibition of acetylcholinesterase activity.

Itopride hydrochloride has a specific effect on the upper gastrointestinal tract, accelerating gastric transit and improving gastric emptying.

Itopride hydrochloride has no effect on serum levels of gastrin.

Pharmacokinetics

Intopride hydrochloride is rapidly and almost completely absorbed in the GI tract. Its relative bioavailability is 60%, which is due to metabolism during first passage through the liver. Food has no effect on bioavailability. The maximum plasma concentration (Cmax) of 0.28 µg/ml is reached 0.5-0.75 h after administration of 50 mg of itopride hydrochloride.

Recurrent oral administration of itopride hydrochloride at a dose of 50-200 mg three times daily for 7 days showed linear pharmacokinetics of the drug and its metabolites, and cumulation was minimal.

Distribution

Itopride hydrochloride is 96% bound to plasma proteins, mainly to albumin. Binding to alpha1-acid glycoprotein is less than 15% of total binding.

Itoprid is actively distributed in the tissues (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. Itoprid penetrates into breast milk.

Metabolism

Itoprid undergoes active biotransformation in the liver in humans. Three metabolites have been identified, only one of which exhibits little activity that has no pharmacological significance (approximately 2-3% of that of itopride). The primary metabolite in humans is N-oxide, which is formed by oxidation of the quaternary amino-N-dimethyl group.

Itoprid is metabolized by the action of flavin-dependent monooxygenase (FMO3). The number and efficiency of FMO isoenzymes in humans can vary depending on the genetic polymorphism, which in rare cases leads to the development of an autosomal recessive condition known as trimethylaminuria (fish-smell syndrome). In patients with trimethylaminuria, the half-life of ithopride is prolonged.

According to in vivo pharmacokinetic studies, itoprid has no inhibitory or inducing effect on CYP2C19 and CYP2E1. Therapy with itopride has no effect on CYP or uridine diphosphate glucuronidyltransferase activity.

Itopride hydrochloride and its metabolites are excreted mainly in the urine. Renal excretion of ithopride and its N-oxide after a single oral administration of the drug in therapeutic doses in healthy subjects was 3.7% and 75.4%, respectively. The terminal period of semi-elimination of itopride hydrochloride is about 6 hours.

Indications

Heartburn, Bloating, Appetite disorders, Vomiting, GI motility disorders, Gastritis, Pelvic pain, Meteorism, NauseaItopride hydrochloride is used for symptomatic treatment of functional non-ulcer dyspepsia (chronic gastritis), in particular for relief of abdominal bloating, rapid satiety, pain or discomfort in the upper abdomen, anorexia, heartburn, nausea and vomiting.

Active ingredient

Itoprid

Composition

1 tablet contains:

The active ingredient:

itopride hydrochloride – 50 mg;

Associates:

Lactose – 34.975 mg (including excess due to loss in weight during manufacture – 2.93%),

corn starch – 15 mg,

carmellose – 20 mg,

Anhydrous silicic acid – 4 mg,

Magnesium stearate – 1 mg,

hypromellose – 4.4 mg,

/p>

macrogol 6000 – 0.4 mg,

titanium dioxide – 0.2 mg,

carnauba wax – 0.025 mg.

How to take, the dosage
How to take, the dosage
Usually adults are prescribed orally 1 tablet of Ganaton 50 mg 3 times a day before meals. Recommended daily dose is 150 mg. The above dose may be reduced taking into account the age of the patient.

Interaction
Interaction
A metabolic interaction is unlikely, because itoprid is metabolized by flavin monooxygenase and not by CYP450.
In concomitant use of warfarin, diazepam, diclofenac sodium, ticlopidine hydrochloride, nifedipine and nicardipine hydrochloride no changes in protein binding were observed.
Itopride increases gastric motility, so it may affect the absorption of other drugs that are prescribed orally. Particular caution should be exercised when using drugs with a low therapeutic index, as well as forms with delayed release of the active substance or drugs with an enteric coating.
The anti-ulcer agents, such as cimetidine, ranitidine, teprenone and cetraxate, do not affect the prokinetic effect of itopride.
Anticholinergic agents may weaken the effects of itopride.

Special Instructions
Special Instructions
With regard to enhancing the isoprid action of acetylcholine, caution should be exercised when prescribing because of the possible development of cholinergic adverse reactions in patients for whom this may aggravate the underlying disease.

Synopsis
Synopsis
White film-coated tablets, round, with a rib on one side and engraved “HC 803” on the other.

Contraindications
Contraindications
high sensitivity to itopride or any excipient of the drug;
patients with gastrointestinal bleeding or mechanical obstruction or perforation;
children (under 16 years of agepatients with gastrointestinal bleeding, mechanical obstruction or perforation;
childhood (under 16 years);
pregnancy and lactation.
Cautious use
Because of the increased isoprid action of acetylcholine, caution should be exercised because of possible cholinergic adverse reactions in the category of patients for whom their occurrence may aggravate the underlying disease.

Side effects
Side effects
Blood and lymphatic system disorders: leukopenia, thrombocytopenia.
Allergic reactions: skin hyperemia, skin itching, rash, anaphylaxis.
Endocrine disorders: increase in prolactin levels, gynecomastia.
Nervous system disorders: dizziness, headache, tremor.
Gastrointestinal disorders: diarrhea, constipation, abdominal pain, increased salivation, nausea, jaundice.
Laboratory changes: increase of aspartate aminotransferase (ACT), alanine aminotransferase (ALT), gammaglutamyl transpeptidase, alkaline phosphatase activity and bilirubin level.

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

Pregnancy use
Pregnancy use
It is recommended to use Ganaton during pregnancy and lactation only when there is no safer alternative and the expected benefits outweigh the possible risks.

Similarities
Similarities
Itomed, Retch

Additional information
Weight 0.031 kg
Shelf life
5 years
Conditions of storage
List B. At the temperature below 25°C, in a dry place protected from light. The drug should be kept out of reach of children.
Manufacturer
Mylan EPD G.K., Japan
Medication form
pills
Brand
Mylan EPD G.K.