Tolperisone Medisorb, 30 pcs., 150 mg, film-coated tablets

Composition and dosage forms

The drug is available in the form of tablets for oral administration: white or cream-colored, biconvex, with a characteristic medicinal odor. Dosage of the active component: 50 and 150 mg.

The active ingredient of the drug is tolperisone hydrochloride, which has a relaxing effect on the fibers of muscle tissue. Each tablet, in addition to the active component, contains auxiliary and formative components:

• lactose;
• lemon acid;
• stearic acid;
• crospovidone.

The drug shell contains: talc, titanium dioxide, polyvinyl chloride and other components.

Mechanism of action of the drug Tolperisone

The drug selectively inhibits the activity of parts of the brain responsible for regulating the motor functions of muscles. It has a central anticholinergic effect, has a slight antispasmodic effect, expands the lumen and reduces vascular tone. Tolperisone does not affect the activity of the peripheral nervous system.

The drug tablets dissolve and are absorbed into the blood in the gastrointestinal tract. Their active component has a bioavailability of about 20%. The effect of the medicine begins 20–30 minutes after administration, reaching a maximum within 1–1.5 hours. The effect lasts 4–5 hours. The medication does not accumulate in the body. All its substances are transformed in the liver. Metabolites are excreted through the kidneys in the urine within 6–8 hours.

Tolperisone Canon (50 and 150 mg)

The safety profile of tolperisone was assessed based on post-marketing data from more than 12,000 patients. According to these data, the most common disorders were skin and subcutaneous tissue disorders, general disorders, and disorders of the nervous system and gastrointestinal tract. During post-marketing use, hypersensitivity reactions accounted for 50 - 60% of all adverse reactions. Most adverse reactions were not serious and went away on their own. Life-threatening hypersensitivity reactions were recorded very rarely. Adverse reactions are listed below according to MedDRA classification and frequency: uncommon (≥1/1,000 to Blood and lymphatic system disorders Very rare:

anemia, lymphadenopathy.
Immune system disorders Rare:
hypersensitivity reaction, anaphylactic reaction;
Very rare:
anaphylactic shock;
Frequency unknown:
angioedema, including swelling of the face and lips.
Metabolic and nutritional disorders Uncommon:
anorexia;
Very rare:
polydipsia.
Mental disorders Uncommon:
insomnia, sleep disorders;
Rarely:
decreased activity, depression;
Very rare:
confusion.
Nervous system disorders Uncommon:
headache, dizziness, drowsiness;
Rarely:
disturbance of attention, tremor, epilepsy, hypoesthesia, paresthesia, lethargy.
Visual disorders Rare:
blurred vision.
Hearing and labyrinthine disorders Rare:
tinnitus, vertigo.
Cardiac disorders Rare:
angina pectoris, tachycardia, palpitations;
Very rare:
bradycardia.
Vascular disorders : Uncommon:
arterial hypotension.
Rarely:
hot flashes.
Disorders of the respiratory system, chest and mediastinal organs Rarely:
shortness of breath, nosebleeds, rapid breathing.
Gastrointestinal disorders Uncommon:
abdominal discomfort, diarrhea, dry mouth, dyspepsia, nausea;
Rarely:
pain in the epigastric region, constipation, flatulence, vomiting.
Disorders of the liver and biliary tract Rarely:
mild liver failure.
Disorders of the skin and subcutaneous tissues Rarely:
allergic dermatitis, increased sweating, itching, urticaria, rash.
Renal and urinary tract disorders Rare:
enuresis, proteinuria.
Musculoskeletal and connective tissue disorders Uncommon:
muscle weakness, myalgia, pain in the extremities;
Rarely:
discomfort in the limbs;
Very rare:
osteopenia.
General disorders and administration site disorders Uncommon:
asthenia, discomfort, fatigue;
Rarely:
feeling of intoxication, feeling of heat, irritability, thirst;
Very rare:
chest discomfort.
Laboratory and instrumental data Rarely:
decreased blood pressure, hyperbilirubinemia, changes in the activity of liver enzymes, thrombocytopenia, leukocytosis;
Very rare:
increased plasma creatinine concentration.
If any of the undesirable reactions indicated in the instructions worsen, or you notice any other undesirable reactions not listed in the instructions, notify your doctor.

For what diseases is Tolperisone indicated?

It is recommended to use the drug in the following conditions:

• increased tone, muscle spasms;
• spastic contractures of the limbs;
• cerebral palsy;
• dysfunction of the spinal cord;
• rigidity, muscle dystonia;
• obliterating sclerosis of the extremities;
• Raynaud's syndrome;
• diabetic angiopathy, thromboangiitis and other manifestations of arterial damage;
• Parkinson's disease;
• acrocyanosis, dysbasia, other painful conditions caused by disorders of vascular innervation;
• disturbances of venous circulation and lymph movement in conditions after thrombosis;
• vascular encephalopathy;
• infantile spastic paralysis;
• trophic ulcers of the lower extremities;
• epilepsy.

The medication is approved for use from the age of 1 year.

When is Tolperisone contraindicated?

It is necessary to refuse treatment with the drug during pregnancy and lactation. There is not enough information about the effect of the active substance on fetal formation. The systemic effect that it causes can affect the condition of both mother and child and cause irreversible disorders.

Other contraindications for use:

• myasthenia gravis;
• individual hypersensitivity to the components of the drug;

Signs of a possible allergic reaction to Tolperisone: bronchospasm, skin itching, urticaria, the appearance of red spots - erythema, anaphylactic shock, Quincke's edema.

Tolperisone tablets p/o 150 mg No. 10x3

Name

Tolperisone tablets 150 mg in container pack No. 10x3

Description

The tablets are white, round, biconvex, film-coated, with a slight characteristic odor.

Main active ingredient

Tolperisone

Release form

Pills

Dosage

150mg

Pharmacological properties

Tolperisone is a drug that acts on the central nervous system. It is used in the treatment of increased muscle tone.

Indications for use

immediate or long-term treatment of pathologically increased skeletal muscle tone in organic neurological diseases (damage to the pyramidal tracts, multiple sclerosis, cerebrovascular disorders, myelopathy, encephalomyelitis, etc.); treatment of muscle hypertonicity and muscle spasms accompanying diseases of the musculoskeletal system (eg spondylosis, spondyloarthritis, cervical and lumbar syndromes, arthrosis of large joints); rehabilitation treatment after surgical interventions in orthopedics and traumatology; treatment of obliterating vascular diseases, as well as syndromes resulting from impaired vascular innervation (for example, acrocyanosis, intermittent angioedema); Specific indications in pediatric practice are Little's disease and other encephalopathies accompanied by muscular dystonia.

Directions for use and doses

Adults The average daily dose, depending on the individual need and tolerance of the drug by the patient, is 150-450 mg, divided into 3 doses. Children The drug is prescribed to children weighing more than 30 kg (over 10 years old) at a daily dose of 2-4 mg/kg body, in 3 divided doses. Considering the low daily doses, when treating children it is recommended to use Tolperisone, film-coated tablets 50 mg. Because The tablets are not intended to be divided into parts; the drug should be prescribed to children weighing 30 kg or more. Use in children Data on the safety and effectiveness of tolperisone in children are limited. Patients with impaired renal function Data on use in patients with impaired renal function are limited. A higher incidence of adverse reactions was observed in this group of patients. Patients with moderate renal impairment require dose titration and careful monitoring. The use of tolperisone is not recommended in patients with severe renal impairment. Patients with impaired liver function Data for use in patients with impaired liver function are limited. A higher incidence of adverse reactions was observed in this group of patients. Patients with moderate hepatic impairment require dose titration and careful monitoring. The use of tolperisone is not recommended in patients with severe liver dysfunction. Directions for use: Use after meals with a glass of water. It is not recommended to take on an empty stomach, as insufficient food may reduce the bioavailability of tolperisone.

Use during pregnancy and lactation

If you are pregnant or breastfeeding, think you are pregnant or are planning a pregnancy, consult your doctor or pharmacist before taking this medicine. Although Tolperisone has not been proven to be toxic to a baby, after a careful risk/benefit assessment, your doctor should decide whether you should use the drug, especially in the first three months of pregnancy. Tolperisone should not be used during pregnancy (especially in the first trimester) unless the expected benefit clearly justifies the potential risk to the fetus. Since there is no data on the excretion of tolperisone in breast milk, the use of this drug is contraindicated during breastfeeding.

Precautionary measures

Hypersensitivity reactions When using drugs containing tolperisone, the development of hypersensitivity reactions was most often reported. Allergic reactions ranged from mild skin reactions to severe systemic reactions, including anaphylactic shock. Symptoms of an allergic reaction: skin redness, rash, urticaria, itching, angioedema (Quincke's edema), tachycardia, hypotension and shortness of breath. Female patients with hypersensitivity reactions to other drugs or a history of allergic reactions are at higher risk. In cases of known hypersensitivity to lidocaine, increased caution should be exercised during the use of tolperisone due to possible cross-reactions. Be alert for any symptoms of hypersensitivity. If symptoms develop, you should immediately stop taking tolperisone and consult a doctor immediately. Patients who have had an episode of hypersensitivity should not re-administer tolperisone. This medicine contains lactose monohydrate. Patients with rare hereditary galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

Interaction with other drugs

If you are taking other medications at the same time, you should consult your doctor. The simultaneous use of tolperisone and the following drugs: thioridazine, tolterodine, venlafaxine, atomoxetine, desipramine, dextromethorphan, metoprolol, nebivolol, perphenazine, may increase the blood levels of these drugs. The bioavailability of tolperisone decreases if taken on an empty stomach. Although tolperisone is a centrally acting drug, its sedative effect is very low. In case of simultaneous administration with other centrally acting muscle relaxants, the dose of tolperisone should be reduced. Tolperisone enhances the effect of niflumic acid, therefore, with simultaneous use, a reduction in the dose of niflumic acid or other non-steroidal anti-inflammatory drugs should be considered.

Contraindications

Hypersensitivity to tolperisone or other similar chemicals (epiresone), as well as to excipients. Myasthenia. Breastfeeding period.

Compound

Each tablet contains: active ingredient: tolperisone hydrochloride - 50 mg or 150 mg; excipients: hydroxypropylcellulose, crospovidone, citric acid monohydrate, stearic acid, colloidal silicon dioxide anhydrous, magnesium stearate, lactose monohydrate, Opadry II (including polyvinyl alcohol, partially hydrolyzed, talc, macrogol 3350 (polyethylene glycol), titanium dioxide E 171).

Overdose

The most common symptoms of overdose are drowsiness, gastrointestinal disorders (nausea, vomiting, epigastric pain), tachycardia, hypertension, bradykinesia and dizziness. Cases of seizures and coma have been reported. There is no specific antidote. Symptomatic treatment is recommended. In case of overdose, consult a doctor immediately!

Side effect

In the post-registration period, the number of messages received about the development of hypersensitivity reactions associated with the use of tolperisone was about 50-60% of all messages received. In most cases these were non-serious adverse reactions. Life-threatening allergic adverse reactions have been reported very rarely. Adverse reactions are listed according to the classification of undesirable side effects in accordance with the damage to organs and organ systems and the frequency of development: very often (? 1/10), often (? 1/100, but

Storage conditions

In a place protected from light and moisture, at a temperature from 15 'C to 25 °C.

Side effects of the drug

During treatment with Tolperisone tablets, the following may appear:

• muscle weakness;
• dyspnea;
• increased fatigue;
• dizziness;
• drowsiness during the daytime;
• decreased blood pressure;
• pain in the stomach and abdominal cavity;
• nausea, vomiting.

In the absence of a serious threat to the physical condition, such symptoms do not require discontinuation of the drug.

Tolperisone Medisorb, 30 pcs., 150 mg, film-coated tablets

The safety profile of tolperisone is confirmed by data from use in more than 12,000 patients. According to these data, the most frequently described disorders are skin and subcutaneous tissue disorders, general disorders, neurological disorders, and gastrointestinal disorders.

During the post-registration period of tolperisone use, the number of reports received about the development of hypersensitivity reactions associated with the use of tolperisone amounted to about 50-60% of all reports received. In most cases these were non-serious adverse reactions. Life-threatening allergic reactions have been reported very rarely.

The frequency of side effects is classified according to the recommendations of the World Health Organization: very often (≥1/10); often (≥1/100,<1/10); uncommon (≥1/1000,<1/100); rare (≥ 1/10000, < 1/1000); very rare (<1/10000), frequency unknown (the incidence of adverse reactions cannot be estimated based on available data).

Disorders of the blood and lymphatic system: very rarely - anemia, lymphadenopathy.

Immune system disorders: rarely - hypersensitivity reactions*, anaphylactic reactions; very rarely - anaphylactic shock.

Metabolic and nutritional disorders: infrequently - anorexia; very rarely - polydipsia.

Mental disorders: infrequently - sleep disturbance, insomnia; rarely - weakness, depression; very rarely - confusion.

Nervous system disorders: uncommon - headache, dizziness, drowsiness; rarely - attention deficit disorder, tremor, epilepsy, paresthesia, convulsions, malaise, lethargy.

Visual disturbances: rarely - decreased visual acuity.

Disorders of the organ of hearing and labyrinth: rarely - tinnitus, vertigo.

Cardiac disorders: rarely - angina pectoris, tachycardia, palpitations; very rarely - bradycardia.

Vascular disorders: infrequently - arterial hypotension; rarely - “flushes” of blood to the face.

Disorders of the respiratory system, chest and mediastinal organs: rarely - shortness of breath, nosebleeds, tachypnea.

Gastrointestinal disorders: uncommon - abdominal discomfort, dyspepsia, diarrhea, dry mouth, nausea; rarely - epigastric pain, constipation, flatulence, vomiting.

Disorders of the liver and biliary tract: rarely - moderate liver failure.

Disorders of the skin and subcutaneous tissues: rarely - allergic dermatitis, hyperhidrosis, itching, skin rash, urticaria.

Muscular, skeletal and connective tissue disorders: uncommon - muscle pain, muscle weakness, pain in the extremities; rarely - discomfort in the limbs; very rarely - osteopenia.

Renal and urinary tract disorders: rarely - enuresis, proteinuria.

General disorders and reactions at the injection site: infrequently - asthenia, feeling of fatigue, malaise; rarely - a feeling of intoxication, a feeling of warmth, irritability, thirst; very rarely - chest discomfort.

Laboratory and instrumental data: rarely - hyperbilirubinemia, liver dysfunction, thrombocytopenia, leukocytosis; very rarely - hypercreatininemia.

*Angioedema, including swelling of the face and lips, has been reported during post-marketing monitoring (frequency unknown).

It is important to report suspected adverse reactions to ensure ongoing monitoring of the benefit-risk relationship of the drug. If you experience any adverse reactions, contact your doctor, pharmacist, or manufacturer. Healthcare professionals are encouraged to report any suspected adverse drug reactions through national adverse reaction reporting systems.

Use of Tolperisone: instructions

The treatment regimen depends on the characteristics of the painful manifestations. General recommendations:

• 1 tablet with a dosage of 50 mg. 2–3 times a day for adults in the first days of therapy;
• 150 mg each. up to three times a day - if the drug is well tolerated in the subsequent period.

For children under 15 years of age, the dosage is selected taking into account body weight:

• 2–4 mg per 1 kg of weight: children from 1 to 6 years old;
• 5 mg per 1 kg. weight: from 7 to 14 years.

The time of eating does not affect the absorption of the drug.

An overdose of the drug is fraught with respiratory problems, cardiac depression, and vascular collapse. It is important to use it strictly as prescribed by the doctor, after carefully studying the instructions. After taking each dose, monitor changes in physical condition.

Tolperisone film-coated tablets 50 mg N30

Tolperisone International nonproprietary name: Tolperisone/Tolperisone. Release form: film-coated tablets 50 mg and 150 mg. Description: round, film-coated tablets, white, biconvex, with a slight characteristic odor.

Composition: each tablet contains: active ingredient: tolperisone hydrochloride - 50 mg or 150 mg; excipients: hydroxypropyl cellulose, crospovidone, citric acid, stearic acid, colloidal anhydrous silicon dioxide, magnesium stearate, lactose monohydrate, Opadry II (including polyvinyl alcohol, partially hydrolyzed, talc, macrogol 3350 (polyethylene glycol ), titanium dioxide E 171).

Pharmacotherapeutic group: Centrally acting muscle relaxants. ATX code: М03ВХ04

Indications for use: immediate or long-term treatment of pathologically increased skeletal muscle tone in organic neurological diseases (damage to the pyramidal tracts, multiple sclerosis, cerebrovascular disorders, myelopathy, encephalomyelitis, etc.); - treatment of muscle hypertonicity and muscle spasms accompanying diseases of the musculoskeletal system (for example, spondylosis, spondyloarthritis, cervical and lumbar syndromes, arthrosis of large joints); — rehabilitation treatment after surgical interventions in orthopedics and traumatology; - treatment of obliterating vascular diseases, as well as syndromes resulting from impaired vascular innervation (for example, acrocyanosis, intermittent angioedema); — specific indications in pediatric practice are Little’s disease and other encephalopathies accompanied by muscular dystonia.

Contraindications Hypersensitivity to tolperisone or other similar chemicals, as well as to auxiliary components. Myasthenia gravis, severe liver and/or kidney dysfunction, pregnancy, lactation. Inside, after eating, without chewing, with a glass of water. The initial dose is 50 mg 2-3 times a day; the dose is gradually increased to 150 mg 2-3 times a day.

Use in pediatrics Data on the safety and effectiveness of tolperisone in children are limited. The drug is prescribed to children weighing more than 30 kg (over 10 years old) at a daily dose of 2-4 mg/kg body weight, in three doses. Patients with impaired renal function

Method of administration and dosage Data on use in patients with impaired renal function are limited. A higher incidence of adverse reactions was observed in this group of patients. Patients with moderate renal impairment require dose titration and careful monitoring. The use of tolperisone is not recommended in patients with severe renal impairment.

Patients with impaired liver function Data for use in patients with impaired liver function are limited. A higher incidence of adverse reactions was observed in this group of patients. Patients with moderate hepatic impairment require dose titration and careful monitoring. The use of tolperisone is not recommended in patients with severe liver dysfunction.

Use after meals with a glass of water. It is not recommended to take on an empty stomach, since insufficient food may reduce the bioavailability of tolperisone.

Side effects Frequency of occurrence of adverse reactions: uncommon (>1/1000 to 1/100 cases); rare (>1/10,000 to 1/1000 cases); very rare (1/10,000 to <10,000 cases). Blood and lymphatic system disorders: very rare: anemia, lymphadenopathy. Immune system disorders: rarely: hypersensitivity reactions, anaphylactic reaction; very rare: anaphylactic shock. Eating and metabolic disorders: uncommon: anorexia; very rare: polydipsia. Mental disorders: uncommon: insomnia, sleep disturbance; rarely: decreased activity, depression. Nervous system disorders: uncommon: headache, dizziness, drowsiness; rarely: disturbance of attention, tremor, convulsions, decreased sensitivity, paresthesia, pathological numbness; very rarely: confusion. Visual disturbances: rarely: blurred vision. Hearing and balance disorders: rarely: tinnitus, dizziness. Cardiac disorders: rarely: angina pectoris, tachycardia, palpitations; very rarely: bradycardia. Cardiovascular system disorders: uncommon: arterial hypotension; rare: pathological blush. Respiratory, thoracic and mediastinal disorders: rarely: dyspnea, epistaxis, tachypnea. Digestive system disorders: uncommon: abdominal discomfort, diarrhea, dry mouth, dyspepsia, nausea; rarely: epigastric pain, constipation, flatulence, vomiting. Hepatobiliary system disorders: rare: mild liver disorders. Skin and subcutaneous tissue disorders: rarely: allergic dermatitis, increased sweating, itching, urticaria, rash. Disorders of the urinary system: rarely: enuresis, proteinuria. Disorders of the musculoskeletal system and connective tissue: uncommon: muscle weakness, myalgia, pain in the extremities; rarely: discomfort in the limbs; very rare: osteopenia. Systemic disorders and complications at the injection site: uncommon: asthenia, malaise, fatigue; rarely: feeling of intoxication, feeling of heat, irritability, thirst; very rare: chest discomfort. Deviations from the norm identified in laboratory tests: rarely: decrease in blood pressure, increase in the concentration of bilirubin in the blood, changes in the activity of liver enzymes, decrease in the number of platelets, increase in the number of leukocytes; very rarely: increased blood creatinine. According to post-marketing data from the use of drugs containing tolperisone, reports of cases of the development of angioedema have been received.

Precautions Hypersensitivity reactions When using drugs containing tolperisone, the development of hypersensitivity reactions was most often reported. Allergic reactions ranged from mild skin reactions to severe systemic reactions, including anaphylactic shock. Symptoms of an allergic reaction: redness of the skin, rash, urticaria, itching, angioedema (Quincke's edema), tachycardia, hypotension and shortness of breath. Female patients with hypersensitivity reactions to other drugs or a history of allergic reactions are at higher risk. In cases of known hypersensitivity to lidocaine, increased caution should be exercised during the use of tolperisone due to possible cross-reactions. Be alert for any symptoms of hypersensitivity. If symptoms develop, you should stop taking tolperisone and consult a doctor immediately. Patients who have had an episode of hypersensitivity should not re-administer tolperisone. This medicine contains lactose monohydrate. Patients with rare hereditary galactose intolerance, Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.

Use during pregnancy and lactation During pregnancy and breastfeeding, the use of the drug is contraindicated. Use during lactation is not recommended, since it is unknown whether tolperisone passes into breast milk.

Effects on the ability to drive vehicles and operate machinery Patients who experience dizziness, drowsiness, impaired attention, convulsions, visual disturbances or muscle weakness after taking the drug should consult a doctor. If these disorders occur, you must refrain from driving a car or working with moving machinery.

Interaction with other drugs The simultaneous use of tolperisone and the following drugs: thioridazine, tolterodine, venlafaxine, atomoxetine, desipramine, dextromethorphan, metoprolol, nebivolol, perphenazine, may increase the blood level of these drugs. The bioavailability of tolperisone decreases if taken on an empty stomach. Although tolperisone is a centrally acting drug, its sedative effect is very low. In case of simultaneous administration with other centrally acting muscle relaxants, the dose of tolperisone should be reduced. Tolperisone enhances the effect of niflumic acid, therefore, with simultaneous use, a reduction in the dose of niflumic acid or other non-steroidal anti-inflammatory drugs should be considered.

Overdose Data on overdose with Tolperisone are scarce. Tolperisone has a wide therapeutic interval. In preclinical acute toxicity studies, high doses caused ataxia, tonic-clonic seizures, dyspnea, and respiratory paralysis. In case of overdose, symptomatic and supportive treatment is recommended. There is no specific antidote.

Packaging 10 tablets in a blister pack; in package No. 10×3.

Storage conditions: Protected from light and moisture, at a temperature from 15 C to 25 C.

Shelf life: 2 years. The medicine cannot be used after the expiration date indicated on the packaging.

Conditions for dispensing from pharmacies By prescription.

special instructions

The therapeutic effect of the drug is enhanced and prolonged when combined with peripheral muscle relaxants, Clonidine, psychoactive and anesthetic agents. Tolperisone reduces the speed of motor skills and mental reactions, affects concentration. During the treatment period, it is necessary to refrain from driving and working with complex mechanisms.

The combination of the drug with alcohol is unacceptable, as it leads to serious intoxication, a sharp decrease in vascular tone, and damage to the central nervous system.