Itomed 50mg 100 trablets — Made in Czech — Free Delivery

Pharmacological properties

Itopride hydrochloride, a d2-type dopamine receptor antagonist, has an anticholinesterase effect. by binding to the d2 receptor, dopamine inhibits the activity of adenylate cyclase in smooth muscle cells of the gastrointestinal tract, which determines its antispasmodic effect. By blocking d2 receptors of dopamine, itopride hydrochloride increases the activity of adenylate cyclase in smooth muscle cells of the gastrointestinal tract, as a result of which the number of cAMPs and energy supply of smooth muscle cells increase. this action gives rise to the activation of motor activity and muscle tone in the gastrointestinal tract.

Acetylcholine interacts with a receptor protein (M3 receptor) in the smooth muscle cell membrane. The receptor protein adenylate cyclase activates an internal receptor, protein kinase, which leads to the phosphorylation of proteins. This process determines an increase in the permeability of the membrane for calcium, which stimulates the contraction of smooth muscles in the gastrointestinal tract. The action of acetylcholine is interrupted by hydrolysis, which occurs under the influence of the enzyme acetylcholinesterase. Itopride hydrochloride, suppressing the activity of acetylcholinesterase, promotes an increase in T½ of endogenous acetylcholine, increases the severity of its action in smooth muscle tissue and stimulates motor activity and tone of the digestive tract.

Itopride hydrochloride, on the basis of its antagonism to the dopamine D2 receptor, has a tonic effect on the smooth muscles of the digestive tract. By suppressing the activity of acetylcholinesterase, it stimulates the motor activity of the stomach in healthy patients and, in case of pathology of a relatively rare and solid fraction, it increases the duration of antral and duodenal contractions, accelerates the evacuation of gastric contents, improves gastroduodenal coordination, and stimulates the passage of intestinal contents.

Together with this, itopride hydrochloride has an antiemetic effect based on its antagonism to dopamine D2 receptors.

Pharmacokinetics. Up to 90% of itopride hydrochloride is absorbed in the intestine. Smax in blood plasma occurs 45 minutes after taking the pill. Food intake does not affect the absorption of itopride hydrochloride. Does not penetrate the BBB and into the cells of the myocardial wiring system.

Undergoes acetylation and oxidation in the liver with the help of flavin-containing monoxidase with the formation of inactive metabolites, which are excreted by the kidneys. T½ of itopride hydrochloride is 6 hours. It is excreted completely within 12 hours after taking a single dose. Not cumulative. Pharmacokinetics of the preparation  within the therapeutic dose is linear.

Indications

Relief of gastrointestinal symptoms of functional non-ulcer dyspepsia (chronic gastritis), namely:

• bloating;
• a feeling of rapid oversaturation;
• pain and discomfort in the upper abdomen;
• heartburn;
• nausea;
• vomit;
• anorexia.

Application

Adults - 1 tablet 3 times a day before meals, without chewing and drinking plenty of water.

The recommended daily dose is 150 mg. It can be reduced taking into account the clinical symptoms, the patient's age.

The duration of treatment is determined by the doctor.

Contraindications

Hypersensitivity to the active substance or any of the components of the preparation. conditions in which an increase in the contractile activity of the gastrointestinal tract can be harmful, for example, bleeding from the digestive tract, obstruction or perforation of the digestive tract; increased plasma prolactin levels.

Side effects

Adverse reactions observed with the use of itopride hydrochloride are classified according to the classes of organs and systems and the frequency of their occurrence: very often (≥1 / 10), often (≥1 / 100, 1/10), sometimes (≥1 / 1000, 1 / 100), rarely (? 1/10 000,1 / 1000), very rarely (1/10 000), including isolated cases.

From the gastrointestinal tract: sometimes - diarrhea, pain in the epigastric region, increased salivation, increased activity of liver enzymes (ALT, ASAT, gamma-glutamyl transpeptidase and alkaline phosphatase); rarely - dry mouth, constipation, jaundice.

From the endocrine system: sometimes - an increase in the level of prolactin in the blood is possible.

From the side of the central nervous system: sometimes - headache, irritability, irritability, insomnia, dizziness, tremor.

On the part of the blood and lymphatic system: rarely - neutropenia, thrombocytopenia; infrequently - leukopenia. If leukopenia develops, it is recommended to stop treatment.

On the part of the skin: rarely - allergic reactions (skin rash, erythema, itching, flushing of the skin), anaphylactic reaction.

From the side of the kidneys and urinary tract: rarely - an increase in the level of creatinine in the blood, urinary retention in patients with prostatic hypertrophy; sometimes - an increase in the level of creatinine in the urine.

Others: infrequently - weakness, back or chest pain, increased fatigue; rarely, gynecomastia or galactorrhea.

special instructions

Elderly people, given the decrease in their liver and kidney function, should be careful when using itopride hydrochloride due to the possible more frequent development of adverse reactions.

It is prescribed with caution to patients with glaucoma and prostate adenoma.

If a dose is missed, it must be taken as soon as possible; do not double the dose if it is time for the next dose.

The preparation contains lactose, therefore, patients with the rarest hereditary forms of galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption syndrome should not use the preparation.

Itopride hydrochloride potentiates the action of acetylcholine and may contribute to cholinergic side effects.

Long-term data are not available.

Use during pregnancy and lactation. The safety of use during pregnancy has not been established, therefore, data on the effect of the preparation on the course of pregnancy and / or fetal development, childbirth and postnatal development are insufficient. In this regard, Itomed is not used during pregnancy.

Itopride hydrochloride passes into the milk of animals when used in therapeutic doses.

The preparation is not recommended for use during breastfeeding.

Children. The preparation is not used in children.

The ability to influence the reaction rate when driving or operating other mechanisms. For the period of treatment, it is recommended to refrain from driving and engaging in potentially hazardous activities that require increased attention and speed of psychomotor reactions, since the preparation can cause dizziness and irritability.

Interactions

Itoprid hydrochloride does not change the activity of the cytochrome p450 enzymatic system, therefore it can be used together with preparations that are metabolized by this system (warfarin, diazepam, diclofenac, ticlopidine, nifedipine, nicardipine, digoxin).

Anticholinergics can reduce the effect of itopride hydrochloride.

The cholinergic effect of itopride can be increased with the simultaneous use of parasymptomatics, as well as cholinesterase inhibitors.

Antiulcer preparations (cimetidine, ranitidine, cetrexate) do not reduce the prokinetic effect of itopride hydrochloride.

Overdose

Overdose cases are not described. gastric lavage and symptomatic treatment are recommended.

Storage conditions

No special storage conditions required.