Relabutin

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT RE LABUTIN (RELABUTIN)

Composition:

Active substance: trimebutine maleate;

One tablet contains 200 mg of trimebutine maleate;

Excipients: lactose monohydrate; pregelatinized starch; hypromellose (hydroxypropylmethylcellulose); sodium starch glycolate (type A); tartaric acid; colloidal anhydrous silicon dioxide; magnesium stearate;

Coating: film-coating mixture Opadry II White (hypromellose; lactose monohydrate; polyethylene glycol (macrogol); titanium dioxide (E 171)).

Pharmaceutical form. Film-coated tablets.

Main physico-chemical characteristics: white or almost white, round, biconvex film-coated tablets.

Pharmacotherapeutic group. Agents used in functional gastrointestinal disorders.

ATC code A03A A05.

Pharmacological properties.

Pharmacodynamics.

Trimebutine is a synthetic agonist of peripheral μ, δ, and κ opioid receptors. Its mechanism of action involves a direct effect on the smooth muscle of the gastrointestinal tract and regulation of motility disorders without affecting the central nervous system. Unlike other opioids, trimebutine does not exhibit selectivity for any of the three receptor types, which allows it to either enhance or inhibit peristalsis. The normalization of motility begins 30 minutes after administration.

Pharmacokinetics.

Absorption

After oral administration, trimebutine is almost completely absorbed. Maximum concentration is reached within 30 minutes.

Distribution

Plasma protein binding is approximately 5%. After oral administration, it crosses the placental barrier in an amount of about 0.05% and passes into breast milk in an amount of about 0.04%.

Metabolism

Trimebutine is metabolized in the liver.

Excretion

It is excreted in the urine as metabolites.

Clinical characteristics.

Indications.

Irritable bowel syndrome; functional gastrointestinal disorders associated with abdominal pain, spasms, sensation of fullness, bloating, constipation, or diarrhea.

Contraindications.

Hypersensitivity to trimebutine or to any of the excipients of the medicinal product.

Interaction with other medicinal products and other forms of interaction.

• Concomitant use of zotepine may prolong anticholinergic effects.
• Trimebutine prolongs the action of d-tubocurarine.
• Trimebutine reduces the effect of cisapride.
• Concomitant administration of trimebutine and procainamide may enhance the vagus nerve's inhibitory effect on myocardial conduction, which may manifest as excessive tachycardia.
• Concomitant use of trimebutine and drugs affecting calcium channels (e.g., calcium channel blockers, captopril, reserpine, midazolam) reduces calcium ion influx, which may suppress intestinal smooth muscle contraction.

Special precautions for use.

The medicinal product Relabutin may cause drowsiness; therefore, it should be used with caution in patients with central nervous system depression.

Relabutin may enhance the sedative effect of medicinal products that depress the central nervous system and/or ethanol.

The medicinal product contains lactose; therefore, it should not be administered to patients with rare hereditary forms of galactose intolerance, lactase deficiency, or glucose-galactose malabsorption syndrome. If you have been diagnosed with intolerance to certain sugars, consult your doctor before taking this medicinal product.

This medicinal product contains less than 1 mmol of sodium (23 mg) per 1 tablet, i.e., it is practically sodium-free.

Use during pregnancy or breastfeeding.

Since data on the use of the drug during pregnancy or breastfeeding are lacking, the drug is contraindicated in women during these periods. Breastfeeding should be discontinued during treatment with this drug.

Ability to influence reaction speed when driving or operating machinery.

If dizziness or drowsiness occurs, refrain from driving or operating machinery.

Dosage and Administration.

Take tablets orally 3 times a day, swallowing them whole with a glass of water.

The single dose for adults is 200 mg (1 tablet); the daily dose is 600 mg (3 tablets).

At the beginning of treatment for irritable bowel syndrome, the maximum daily dose for adults may be 600 mg (3 tablets) divided into 3 doses (i.e., 1 tablet 3 times a day) if necessary.

The duration of treatment is determined individually by the physician. Typically, the treatment course lasts 2–6 weeks, depending on the severity and course of the disease.

Children.

Experience with the use of the drug in children is limited; therefore, it should not be prescribed to this patient group.

Overdose.

There are no data regarding cases of trimbutine overdose. Overdose may enhance the manifestations of adverse reactions.

Adverse Reactions

Adverse effects associated with the use of trimebutine are grouped according to the MedDRA classification.

Frequency is defined as follows: very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1000 to <1/100); rare (≥1/10000 to <1/1000); very rare (<1/10000); not known (frequency cannot be estimated from available data).

Immune system disorders: not known – hypersensitivity reactions (pruritus, urticaria, angioedema, and in exceptional cases anaphylactic shock).

Psychiatric disorders: very rare – anxiety.

Nervous system disorders: common – drowsiness, lethargy, fatigue, dizziness, sensation of heat or cold, headache, apathy.

Ear and labyrinth disorders: very rare – hearing impairment.

Cardiac disorders: rare – cardiac arrhythmias.

Gastrointestinal disorders: common – dry mouth, taste disturbances, diarrhea, dyspepsia, upper abdominal pain, oral numbness, nausea, vomiting, constipation, thirst sensation.

Hepatobiliary disorders: rare – liver function abnormalities; very rare – hepatitis.

Skin and subcutaneous tissue disorders: uncommon – rash; very rare – pruritus, urticaria, erythema, vesicles, papules, exudation, polymorphic erythema; not known – generalized maculopapular rash, erythema, eczematous reactions, and exceptionally severe skin reactions including cases of acute generalized exanthematous pustulosis (AGEP), erythema multiforme, febrile toxidermia.

Renal and urinary disorders: very rare – urinary retention.

Reproductive system and breast disorders: very rare – menstrual cycle disturbances, painful breast enlargement in women, gynecomastia in men.

Investigations: rare – increased levels of liver enzymes (ALT, AST).

Reporting of suspected adverse reactions

Reporting suspected adverse reactions after medicinal product registration is important. It allows ongoing monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals, as well as patients or their legal representatives, should report all suspected adverse reactions and lack of efficacy via the Automated Pharmacovigilance Information System at: https://aisf.dec.gov.ua.

Shelf life.

3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C.

Keep out of reach and sight of children.

Packaging.

10 tablets in a blister; 3 blisters per carton.

Prescription status.

Prescription only.

Manufacturer.

JSC "KYIV VITAMIN PLANT".

Manufacturer's address and place of business.

04073, Ukraine, Kyiv, Kopilivska St., 38.

Web-site: www.vitamin.com.ua