Mebespalin retard (Tablets) Instructions for Use

Marketing Authorization Holder

Atoll LLC (Russia)

Manufactured By

Ozon, LLC (Russia)

Contact Information

OZON LLC (Russia)

ATC Code

A03AA04 (Mebeverine)

Active Substance

Mebeverine (Rec.INN registered by WHO)

Dosage Form

Mebespalin retard

Extended-release film-coated tablets, 200 mg: 7, 10, 14, 20, 21, 25, 28, 30, 35, 40, 42, 45, 49, 50, 56, 60, 63, 70, 75, 80, 90, 100, 105, 120, 125, 140, 150, 160, 175, 180, 200, 210, 225, 240, 250, 270, or 300 pcs.

Dosage Form, Packaging, and Composition

Extended-release film-coated tablets white or almost white, round, biconvex; on the cross-section – a core of white or yellowish-white color.

Excipients: hypromellose, magnesium stearate, colloidal silicon dioxide.

Shell composition: hypromellose, titanium dioxide, macrogol 4000.

7 pcs. – blister packs (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) – cardboard packs.
10 pcs. – blister packs (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) – cardboard packs.
15 pcs. – blister packs (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) – cardboard packs.
20 pcs. – blister packs (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) – cardboard packs.
25 pcs. – blister packs (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) – cardboard packs.
30 pcs. – blister packs (1, 2, 3, 4, 5, 6, 7, 8, 9, 10) – cardboard packs.

Clinical-Pharmacological Group

Myotropic antispasmodic

Pharmacotherapeutic Group

Drugs for the treatment of functional gastrointestinal disorders; synthetic anticholinergic agents, esters with a tertiary amino group

Pharmacological Action

It is a myotropic antispasmodic that has a direct effect on the smooth muscles of the gastrointestinal tract without affecting normal intestinal peristalsis. Multiple mechanisms, such as reducing the permeability of ion channels, blocking the reuptake of norepinephrine, local anesthetic action, and changing water absorption, can cause the local effect of mebeverine on the gastrointestinal tract, but the exact mechanism of action is not known.

Through these mechanisms, Mebeverine has an antispasmodic effect, normalizing intestinal peristalsis and not causing persistent relaxation of gastrointestinal smooth muscle cells (hypotonia). Systemic side effects, including anticholinergic ones, are absent.

The duration of use of the drug is not limited. During the first 2-4 weeks of therapy, a sustained improvement in symptoms is noted. The most pronounced effectiveness can be observed after 6-8 weeks of therapy. When choosing the duration of the course of therapy, it is necessary to take into account the individual characteristics of the disease and the severity of symptoms.

To further improve the symptoms of the disease, it is recommended to continue treatment under medical supervision for 12 months with a continuous therapy regimen or for 6 months with “on-demand” therapy.

The results of clinical studies confirmed an improvement in gastrointestinal symptoms and the quality of life of patients within 2-4 weeks, with further improvement when treatment was extended to 6-8 weeks.

Pharmacokinetics

Absorption

Mebeverine is rapidly and completely absorbed after oral administration.

Distribution

No significant accumulation occurs with repeated doses of the drug.

Metabolism

Mebeverine hydrochloride is mainly metabolized by esterases, which at the first stage split the ester into veratric acid and mebeverine alcohol. The main metabolite circulating in plasma is demethylated carboxylic acid. The T_1/2 of demethylated carboxylic acid at steady state is approximately 2.45 h. With repeated doses, the C_max of demethylated carboxylic acid in the blood is 1670 ng/ml, and the T_max of demethylated carboxylic acid in the blood is 1 h.

Excretion

Mebeverine as such is not excreted from the body but is completely metabolized; its metabolites are almost completely excreted from the body. Veratric acid is excreted by the kidneys. Mebeverine alcohol is also excreted by the kidneys, partly as carboxylic acid and partly as demethylated carboxylic acid.

Indications

• Symptomatic treatment of pain, spasms, dysfunction and discomfort in the intestinal area associated with irritable bowel syndrome;
• Symptomatic treatment of spasms of the gastrointestinal tract organs (including those caused by organic diseases).

ICD codes

Dosage Regimen

For oral administration. The tablets should be swallowed with a sufficient amount of water (at least 100 ml). The tablets should not be chewed, as their coating provides prolonged release of the drug.

Adults – 1 tab. 2 times/day, approximately 20 minutes before meals.

At the beginning of the drug use, the duration of therapy should be at least 6-8 weeks in order to adequately assess the effectiveness of treatment. The duration of use of the drug is not limited. If the patient forgot to take one or more doses, the drug should be continued with the next dose. One or more missed doses should not be taken in addition to the regular dose.

Special patient groups

Studies of the dosage regimen in elderly patients, patients with renal and/or hepatic impairment have not been conducted. Available data from post-registration use of the drug did not reveal specific risk factors for its use in elderly patients and patients with renal and/or hepatic impairment. No change in the dosage regimen is required for elderly patients and patients with renal and/or hepatic impairment.

Adverse Reactions

Reports of the listed side effects were spontaneous, and there is insufficient data for an accurate assessment of the frequency of cases.

Allergic reactions were observed mainly from the skin, but other manifestations of allergy were also noted.

The frequency of adverse reactions is presented according to the following gradation: very common (≥1/10); common (≥1/100, but <1/10); uncommon (≥1/1000, but <1/100); rare (≥1/10000, but <1/1000); very rare (<1/10000); frequency unknown (cannot be estimated from the available data).

From the immune system: frequency unknown – hypersensitivity reactions (anaphylactic reactions – serious allergic reactions that may include: difficulty breathing, rapid pulse, sharp decrease in blood pressure (weakness and dizziness), sweating).

From the skin and subcutaneous tissues: frequency unknown – urticaria (allergic rash), angioedema (serious allergic reaction that may include: difficulty breathing, swelling of the face, neck, lips, tongue, throat), facial edema, exanthema (skin rash).

If any side effects are noted, including those not listed in this instruction, the patient should stop taking Mebespalin retard and immediately consult a doctor.

Contraindications

• Hypersensitivity to any component of the drug;
• Pregnancy;
• Breastfeeding period;
• Age under 18 years.

Use in Pregnancy and Lactation

Pregnancy

There are only very limited data on the use of mebeverine in pregnant women. Animal studies data are insufficient to assess reproductive toxicity. It is not recommended to use Mebespalin retard during pregnancy.

Breastfeeding period

Information on the excretion of mebeverine or its metabolites into breast milk is insufficient. Studies on the excretion of mebeverine into milk in animals have not been conducted.

Mebespalin retard should not be taken during breastfeeding.

Fertility

There are no clinical data on the effect of the drug on fertility in men or women, but known animal studies have not demonstrated adverse effects of mebeverine.

Use in Hepatic Impairment

No change in the dosage regimen is required for patients with hepatic impairment.

Use in Renal Impairment

No change in the dosage regimen is required for patients with renal impairment.

Pediatric Use

The use of the drug is contraindicated under the age of 18 years.

Geriatric Use

No change in the dosage regimen is required for elderly patients.

Special Precautions

Before taking Mebespalin retard, it is necessary to consult a doctor, in case

• If the symptoms of the disease have occurred for the first time;
• Of unintentional and unexplained weight loss;
• Anemia;
• Rectal bleeding or blood in the stool;
• Fever;
• If someone in your family has been diagnosed with colon cancer, celiac disease or inflammatory bowel disease;
• Age over 50 years, and if the symptoms of the disease have occurred for the first time;
• Recent use of antibiotics.

The patient should consult a doctor if the condition worsens while taking the drug or if there is no improvement in symptoms after 2 weeks of use.

Effect on the ability to drive vehicles and mechanisms

Studies on the effect of mebeverine on the ability to drive a car and other mechanisms have not been conducted. The pharmacological properties of mebeverine, as well as the experience of its use, do not indicate any adverse effect on the ability to drive a car and other mechanisms.

Overdose

In case of an overdose of Mebespalin retard, it is necessary to immediately consult a doctor.

Symptoms: theoretically, in case of an overdose, an increase in CNS excitability is possible. In cases of mebeverine overdose, symptoms were either absent or minor and, as a rule, quickly reversible. The observed overdose symptoms were of a neurological and cardiovascular nature.

Treatment: a specific antidote is unknown. Symptomatic treatment is recommended. Gastric lavage is necessary only if intoxication is detected within approximately 1 hour after taking several doses of the drug. Measures to reduce the level of absorption are not required.

Drug Interactions

Only studies on the interaction of mebeverine with alcohol have been conducted. Animal studies have demonstrated no interaction between mebeverine and ethyl alcohol.

Storage Conditions

The drug should be stored in a light-protected place, out of the reach of children, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years. Do not use after the expiration date printed on the package.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.