Itomed (Itoprid)

Active substance: 

itoprida hydrochloride 50 mg;

Excipients:

 lactose monohydrate - 74.68 mg;

pregelatinized corn starch - 5 mg;

croscarmellose sodium - 1.8 mg;

colloidal silicon dioxide - 1 mg;

magnesium stearate - 2.52 mg; 

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)

Itomed - stimulating tone and motility of the gastrointestinal tract, antiemetic.

Pharmacodynamics

Enhances gastrointestinal motility due to antagonism with D ₂ -dopamine receptors and inhibition of acetylcholinesterase. It activates the release of acetylcholine, inhibits its destruction.

It has an antiemetic effect due to interaction with D ₂ receptors located in the trigger zone. Causes dose-dependent inhibition of apomorphine-induced vomiting.

It activates the propulsive motility of the stomach due to antagonism with D ₂ receptors and dose-dependent inhibition of acetylcholinesterase activity.

It has a specific effect on the upper gastrointestinal tract, accelerates transit through the stomach, and improves its emptying. It does not affect the serum concentration of gastrin.

Pharmacokinetics

Quickly and well absorbed in the digestive tract. The relative bioavailability of the drug is 60%. C _max  - 0.28 μg / ml, after taking 50 mg of the drug T _max  in plasma - about 0.5–0.75 hours. With repeated use of 50–200 mg 3 times a day within 7 days, the pharmacokinetics is linear, cumulation is minimal.

It binds to plasma proteins (mainly with albumin) by 96%, with α ₁ -acid glycoprotein by less than 15%. It is actively distributed in tissues (V _d  - 6.1 l / kg) and is found in high concentrations in the kidneys, small intestine, liver, adrenal glands, and stomach. In therapeutic doses, it slightly penetrates the brain and spinal cord, breast milk.

It is metabolized in the liver under the influence of flavin-dependent monooxygenase. 3 metabolites were identified, one of which exhibits insignificant activity: 2-3% of the activity of itopride.

It is excreted by the kidneys. T _1/2  is 6 hours, in patients with trimethylaminuria, T _1/2  is increased.

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

• flatulence;
• gastralgia;
• discomfort in the epigastric region;
• anorexia;
• heartburn;
• nausea;
• vomiting

Itopride is contraindicated in pregnancy.

When taking the drug in therapeutic doses, itopride slightly penetrates into breast milk, so you should stop taking the drug during breastfeeding (see "Contraindications").

• hypersensitivity to itoprid or any auxiliary component of the drug;
• gastrointestinal bleeding, mechanical obstruction and perforation of the gastrointestinal tract;
• lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
• pregnancy;
• lactation period;
• children's age (up to 16 years);

With caution: patients taking cholinesterase inhibitors and m-cholinomimetics, as well as elderly patients with reduced liver and kidney function.

From the hemopoietic organs: leukopenia, thrombocytopenia.

From the endocrine system: gynecomastia, hyperprolactinemia.

From the digestive system: increased salivation, nausea, diarrhea, constipation, jaundice, pain in the epigastric region.

From the nervous system: headache, sleep disturbance, irritability, dizziness, tremor.

Allergic reactions: urticaria, anaphylactic shock.

Laboratory indicators: increased activity of AST, ALT, GGT, alkaline phosphatase, hyperbilirubinemia.

Accelerates the absorption of other drugs.

The prokinetic effect of the drug does not change under the influence of agents that reduce the acidity of gastric juice (cimetidine, ranitidine, teprenone, cetraxate).

M-anticholinergic drugs lower the effectiveness of itopride.

The cholinergic effect of itopride may increase while taking m-cholinomimetics, as well as cholinesterase inhibitors.

Inside, 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 was not taken on time, then in the future it should be taken at regular intervals.

It is not recommended to take in a double dose to compensate for the missed.

Treatment: gastric lavage and symptomatic therapy.

If symptoms of galactorrhea and gynecomastia manifest, it is necessary to interrupt or completely discontinue treatment.

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

Influence on the ability to drive vehicles or perform work requiring an increased rate of physical and mental reactions. During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.