Trimedat, 152, 5 g

Pharmacotherapeutic group: antispasmodic agent

ATC code: A03AA05

Pharmacological properties

Pharmacodynamics<

Trimebutin, acting on the encephalinergic system of the intestine, is a regulator of its peristalsis. Acting on peripheral δ-, μ- and k-receptors, including those located directly on the smooth muscles throughout the gastrointestinal (GI) tract, it regulates motility without affecting the central nervous system. Thus, trimebutine restores normal physiological activity of gastrointestinal musculature (esophagus, stomach, intestines, biliary tract) in various GIT diseases associated with motility disorders (has a stimulating effect in hypokinetic states and spasmolytic in hyperkinetic states).

Normalizing visceral sensitivity, trimebutine provides analgesic effect in abdominal pain syndrome.

Pharmacokinetics

Trimebutin is rapidly absorbed from the GI tract after oral administration. Maximum concentration (C_max) in blood plasma is reached after 1-2 hours. Bioavailability is 4-6%. Volume of distribution (V_d) is 88 l. The degree of binding to plasma proteins is low – about 5%. Trimebutine penetrates through the placental barrier to a small extent. Trimebutine is biotransformed in the liver and excreted in the urine mainly as metabolites (about 70% during the first 24 hours). The active metabolite of trimebutine is desmethyltrimebutine. The elimination half-life (T_1/2) is about 12 h.

Indications

Symptomatic treatment of pain, abdominal cramps and discomfort, bloating (flatulence), bowel motor disorders with changes in stool frequency (diarrhea or constipation), dyspepsia, heartburn, belching, nausea, vomiting, associated with functional diseases of the gastrointestinal tract and biliary tract (non-erosive form of gastroesophageal reflux disease, biliary stone disease, biliary tract dysfunction, irritable bowel syndrome, sphincter Oddi dysfunction, postcholecystectomy syndrome). Postoperative paralytic intestinal obstruction.

Active ingredient

Trimebutin

Composition

Active ingredient: trimebutin – 1.2 g;

Auxiliary substances: sucrose, poloxamer 188 (micronized), polysorbate-80, betacarotene, orange flavoring.

How to take, the dosage

Ingestion.

Before using the powder for suspension preparation, dilute it with potable water at room temperature up to the mark on the bottle, shake thoroughly until a homogeneous suspension is obtained, add potable water at room temperature again up to the mark. Before each intake of the drug the contents of the bottle should be shaken thoroughly until a homogeneous suspension is obtained.

The required dose is measured using the measuring cup included in the package, which has special graduations with prices corresponding to the amount of the drug in milligrams (from 25 mg to 100 mg). After use the measuring cup is washed with running water, dried and stored together with the bottle.

Adults and children from 12 years old take 100-200 mg 3 times a day.

Children 5-12 years: 50 mg 3 times a day.

Children 3-5 years: 25 mg 3 times a day.

In order to prevent relapse of irritable bowel syndrome after the course of treatment (4 weeks) it is recommended to continue taking the drug at a dose of 300 mg daily for 12 weeks during remission.

Interaction

No drug interactions have been described.

Special Instructions

The course of treatment of irritable bowel syndrome in the acute period at a dose of 600 mg per day for 4 weeks and continuation of treatment after the course at a dose of 300 mg per day for 12 weeks avoids recurrence of the disease.

Patients with diabetes should pay attention to the sucrose content of the drug. One single dose of the ready-to-use suspension containing 25 mg of the active ingredient contains 3.1 g of sucrose, which corresponds to 0.3 bread units (BE).

Influence on ability to drive vehicles, mechanisms

The drug has no sedative effect, does not affect the speed of psychomotor reaction and can be used in various professions, including those requiring increased attention and coordination of movements. However, given the possible side effects which may affect the above abilities (dizziness and others), caution should be exercised when driving motor vehicles and engaging in other potentially dangerous activities.

Synopsis

White or almost white crystalline powder with orange odor. The presence of single specks of red color is allowed.

Contraindications

Hypersensitivity to the ingredients of the drug.

Sugar/isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption.

Children under 3 years of age.

Pregnancy.

Cautions

Patients with diabetes mellitus should exercise caution due to the presence of sucrose in the drug (see “Special Precautions” section).

The drug should be used with caution during breastfeeding because there is no data about its ability to penetrate into the breast milk.

Side effects

The side effects listed below are presented according to the following frequency gradations: Very common (≥1/10); common (≥1/100, < 1/10); infrequent (≥1/1000, < 1/100); rare (≥1/10000, < 1/1000); very rare (< 1/10000) (including individual reports); frequency unknown (no data available to determine incidence).

Digestive system disorders: frequency unknown – dry mouth, unpleasant taste, diarrhea, dyspepsia, nausea, constipation.

Allergic reactions: incidence unknown – skin rash.

Nervous system disorders: frequency unknown – drowsiness, fatigue, dizziness, headache, anxiety.

Urogenital system disorders: frequency unknown – menstrual disorders, urinary retention.

Others: frequency unknown – painful enlargement of the breasts.

Overdose

No cases of overdose during trimebutine administration have been registered so far. Treatment: withdrawal of the drug, gastric lavage, administration of activated charcoal, symptomatic therapy. There are no specific antidotes.

Pregnancy use

No data on teratogenicity and embryotoxicity of trimebutine have been found in experimental studies. Nevertheless, due to the lack of necessary clinical data, the use of the drug during pregnancy is contraindicated. It is not recommended to prescribe the drug during lactation due to the lack of reliable clinical data confirming the safety of use during this period. If it is necessary to use the drug during breastfeeding, breastfeeding should be stopped.

Similarities

Trimedat, Trimedat for children, Neobutin retard, Trimedat Forte