Itomed, 50 mg 40 pcs.

Itomed – stimulates gastrointestinal tone and motility, antiemetic.

Pharmacodynamics

It enhances gastrointestinal motility due to antagonism with D₂-dopamine receptors and inhibition of acetylcholinesterase. Activates the release of acetylcholine and inhibits its degradation.

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

Activates propulsive gastric motility through antagonism with D₂-receptors and dose-dependent inhibition of acetylcholinesterase activity.

It has a specific effect on the upper gastrointestinal tract, accelerates gastric transit and improves gastric emptying. It has no effect on serum concentrations of gastrin.

Pharmacokinetics

It is quickly and well absorbed in the gastrointestinal tract. The relative bioavailability of the drug is 60%.C_max is 0.28 mcg/mL, after administration of 50 mg of the drug T_max in plasma is about 0.5-0.75 h. When repeatedly administered 50-200 mg 3 times daily for 7 days, pharmacokinetics is linear and cumulation is minimal.

It binds with plasma proteins (mainly with albumin) by 96%, with α₁-acid glycoprotein by less than 15%. It is actively distributed in tissues (V_d – 6.1 l/kg) and found in high concentrations in the kidneys, small intestine, liver, adrenal glands, stomach. In therapeutic doses it slightly penetrates into brain and spinal cord, breast milk.

It is metabolized in the liver under the action of flavin-dependent monooxygenase. Three metabolites have been identified, one of which has negligible activity: 2-3% of the activity of ithopride.

Extracted by the kidneys. T_1/2 is 6 h, in patients with trimethylaminuria T_1/2 is increased.

Indications

Symptomatic treatment of functional non-ulcer dyspepsia (chronic gastritis):

Active ingredient

Composition

Active substance:

itopride hydrochloride50 mg;

Ancillary substances:

Lactose monohydrate – 74.68 mg;

Pregelatinized corn starch – 5 mg;

Croscarmellose sodium – 1.8 mg;

Colloidal silica – 1 mg;

Magnesium stearate – 2.52 mg;

Film film sheath:

Opadry 85F18422 white – 3 mg (polyvinyl alcohol, partially hydrolyzed – 1.2 mg, titanium dioxide – 0.75 mg, macrogol 4000 – 0.606 mg, talc – 0.444 mg)

How to take, the dosage

Ingestion, before meals, 1 tablet 3 times a day.

The daily dose of the drug is 3 tablets (150 mg).

In elderly patients the dose is reduced.

If the drug is not taken on time, it should be taken at regular intervals thereafter.

It is not recommended to take a double dose to make up for a missed dose.

Interaction

Accelerates absorption of other drugs.

The prokinetic effect of the drug is not affected by agents that reduce gastric acidity (cimetidine, ranitidine, teprenone, cetraxate).

M-cholinoblockers decrease the effectiveness of itopride.

The cholinergic effects of itopride may be increased by concomitant administration of m-cholinomimetics as well as cholinesterase inhibitors.

Special Instructions

In case of symptoms of galactorrhea and gynecomastia, treatment should be interrupted or discontinued completely.

In treatment of primary biliary cirrhosis, transient decompensation of cirrhosis of the liver may be observed, which disappears after discontinuation of the drug.

Impact on the ability to drive vehicles or perform work requiring increased speed of physical and mental reactions.

During treatment, it is necessary to refrain from driving and engaging in potentially hazardous activities requiring increased concentration and rapid psychomotor reactions.

Contraindications

Side effects

Blood organs: leukopenia, thrombocytopenia.

Endocrine system disorders: gynecomastia, hyperprolactinemia.

Digestive system disorders: increased salivation, nausea, diarrhea, constipation, jaundice, epigastric pain.

Nervous system disorders: headache, sleep disturbance, irritability, dizziness, tremor.

Allergic reactions: urticaria, anaphylactic shock.

Laboratory measures: increase in AST, ALT, GGT, ALF, hyperbilirubinemia.

Overdose

Treatment: gastric lavage and symptomatic therapy.

Pregnancy use

Itoprid is contraindicated in pregnancy.

Itopride slightly penetrates into breast milk when taking the drug in therapeutic doses, therefore the drug should be discontinued during breastfeeding (see “Contraindications”).

Similarities