Mebespalin (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

Film-coated tablets, 135 mg: 10, 20, 25, 30, 40, 50, 60, 75, 80, 90, 100, 120, 125, 150, 200, 250, or 300 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, round, biconvex; the cross-section shows a core of white or almost white color.

Excipients: lactose monohydrate (milk sugar), potato starch, talc, povidone K25, magnesium stearate.

Shell composition: hypromellose, titanium dioxide, macrogol 4000.

10 pcs. – contour cell packs (1, 2, 3, 4, 5, 10) – cardboard packs.
20 pcs. – contour cell packs (1, 2, 3, 4, 5, 10) – cardboard packs.
25 pcs. – contour cell packs (1, 2, 3, 4, 5, 10) – cardboard packs.
30 pcs. – contour cell packs (1, 2, 3, 4, 5, 10) – cardboard packs.
10 pcs. – jars (1) – cardboard packs.
20 pcs. – jars (1) – cardboard packs.
25 pcs. – jars (1) – cardboard packs.
30 pcs. – jars (1) – cardboard packs.
40 pcs. – jars (1) – cardboard packs.
50 pcs. – jars (1) – cardboard packs.
100 pcs. – jars (1) – cardboard packs.

Clinical-Pharmacological Group

Myotropic antispasmodic

Pharmacotherapeutic Group

Spasmolytic agent

Pharmacological Action

Myotropic antispasmodic, has a direct effect on the smooth muscles of the gastrointestinal tract without affecting normal intestinal peristalsis.

The exact mechanism of action is unknown, but multiple mechanisms, such as reducing ion channel permeability, blocking norepinephrine reuptake, local anesthetic action, and altering water absorption, may cause the local effect of mebeverine on the gastrointestinal tract.

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 drug use is not limited. A sustained improvement in symptoms is noted within the first 2-4 weeks of therapy. The most pronounced effectiveness may be observed after 6-8 weeks of therapy.

When choosing the duration of the treatment course, individual characteristics of the disease course and severity of symptoms must be taken into account.

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

Clinical study results confirmed improvement in gastrointestinal symptoms and patient quality of life within 2-4 weeks, with further improvement upon extending treatment 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 initially cleave the ester into veratric acid and mebeverine alcohol. The main metabolite circulating in plasma is the demethylated carboxylic acid. The T_1/2 at steady state of the demethylated carboxylic acid is approximately 2.45 h. With repeated doses, the C_max of the demethylated carboxylic acid in blood is 1670 ng/ml, and the T_max of the demethylated carboxylic acid in blood is 1 h.

Excretion

Mebeverine as such is not excreted from the body but is completely metabolized; its metabolites are almost completely eliminated 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.

Symptoms may include: abdominal pain, cramps, feeling of bloating and flatulence, change in stool frequency (diarrhea, constipation, or alternating diarrhea and constipation), change in stool consistency.

ICD codes

Dosage Regimen

Orally. The tablets should be swallowed without chewing, with a sufficient amount of water (at least 100 ml).

Adults – 1 tab. 3 times/day, approximately 20 minutes before meals.

At the beginning of drug use, the duration of therapy should be at least 6-8 weeks to adequately assess treatment effectiveness. The duration of drug administration is not limited.

If the patient forgot to take one or more doses, drug administration 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 dosing regimen in elderly patients, patients with renal and/or hepatic impairment have not been conducted. Available post-registration data on drug use did not reveal specific risk factors for its use in elderly patients and patients with renal and/or hepatic impairment.

No dosage regimen adjustment 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.

From the skin: urticaria (allergic rash), angioedema (serious allergic reaction which may include: difficulty breathing, swelling of the face, neck, lips, tongue, throat), facial edema, exanthema (skin rash).

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

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

Contraindications

• Hypersensitivity to mebeverine and/or to any of the excipients of the drug;
• Congenital lactose intolerance, lactase deficiency, glucose-galactose malabsorption syndrome;
• 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 study data are insufficient to assess reproductive toxicity. It is not recommended to use Mebeverine 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. Mebeverine should not be taken while breastfeeding.

Fertility

Clinical data on the effect of the drug on fertility in men or women are lacking, however, known animal studies have not demonstrated adverse effects of mebeverine.

Use in Hepatic Impairment

No dosage regimen adjustment is required for patients with hepatic impairment.

Use in Renal Impairment

No dosage regimen adjustment 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 dosage regimen adjustment is required for elderly patients.

Special Precautions

Before taking mebeverine, the patient should 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 the patient’s family has been diagnosed with colon cancer, celiac disease, or inflammatory bowel disease;
• If the patient is over 50 years old and if the symptoms of the disease have occurred for the first time;
• Recent use of antibiotics.

The patient must consult a doctor if their 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 the drug, as well as the experience of its use, do not indicate any adverse effect of mebeverine on the ability to drive a car and other mechanisms.

Overdose

In case of mebeverine overdose, it is necessary to immediately consult a doctor.

Symptoms: theoretically, in case of 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 neurological and cardiovascular in 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 this drug with alcohol have been conducted. Animal studies demonstrated no interaction between mebeverine and ethyl alcohol.

Storage Conditions

The drug should be stored 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 packaging.

Dispensing Status

The drug is available without a 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.