Itopra, 50 mg 40 pcs.

A drug that stimulates gastrointestinal motility. Itopride increases propulsive motility of the gastrointestinal tract due to antagonism to dopamine D2-receptors and dose-dependent inhibition of acetylcholinesterase activity. Itopride activates the release of acetylcholine and inhibits its degradation.

Itopride has a specific effect on the upper gastrointestinal tract, accelerating gastric transit and improving gastric emptying. It also has an antiemetic effect due to interaction with D2-receptors located in the trigger zone. Itopride caused dose-dependent suppression of apomorphine-induced vomiting. It has no effect on serum levels of gastrin.

It is rapidly and well absorbed in the gastrointestinal tract. The relative bioavailability is 60%. Cmax – 0.28 µ/ml, TSmax – 0.5-0.75 h after administration of 50 mg of the preparation. When repeated administration of 50-200 mg 3 times daily for 7 days the pharmacokinetics is linear, cumulation is minimal.

Protein binding is 96% (mainly with albumin; with alpha1 acid glycoprotein – less than 15%). It is distributed in the kidneys, small intestine, liver, adrenal glands, stomach. Distribution volume is 6.1 l/kg. In therapeutic doses slightly penetrates into the brain and spinal cord, into breast milk. It is metabolized in liver under the action of flavin-dependent monooxygenase.

The 3 metabolites are identified, only one of them has negligible activity (2-3% of the activity of ithopride), which has no pharmacological significance. It is excreted by the kidneys. T1/2 is 6 h, in patients with trimethylaminuria T1/2 is increased.

Indications

Symptomatic treatment of functional non-ulcer dyspepsia (chronic gastritis), in particular – relief of bloating (flatulence), pain or discomfort in the epigastric region (gastralgia), anorexia, heartburn, nausea, vomiting, feelings of rapid satiety.

Active ingredient

Composition

Active ingredient:

itopride hydrochloride 50.0 mg.

How to take, the dosage

It is taken orally in 50 mg 3 times a day.

The recommended daily dose is 150 mg.

The stated dose can be reduced according to the patient’s age.

Interaction

Accelerates absorption of other drugs.

The prokinetic effect of the drug is not changed under the influence of anti-ulcer agents (cimetidine, ranitidine, teprenone, cetraxate).

Cholinergic drugs weaken the effect of the drug.

Special Instructions

With caution, itoprid should be used in patients for whom the occurrence of cholinergic adverse reactions (associated with increased acetylcholine action under the influence of itoprid) may worsen the course of the underlying disease.

Contraindications

High sensitivity to itopride or any excipient of the drug, gastrointestinal bleeding, mechanical obstruction and perforation of the gastrointestinal tract, children under 16 years of age, pregnancy and lactation (breast-feeding).

Side effects

Hematopoietic system: Leukopenia, thrombocytopenia.

From the endocrine system: increased prolactin levels, gynecomastia.

CNS side:dizziness, headache, tremor.

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

Allergic reactions:skin hyperemia, skin itching, rash, anaphylaxis.

Similarities