Active substanceTolmoreysonTolmoreyson
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  • Dosage form: & nbspTOthe apsules.
    Composition:

    One 50 mg capsule contains:

    Active substance: tollerizon hydrochloride -50.00 mg;

    Excipients: cellulose microcrystalline - 55.22 mg; lactose monohydrate (sugar milk) - 34.33 mg; croscarmellose sodium - 6.32 mg; hypromellose - 1.58 mg; citric acid monohydrate - 1.50 mg; magnesium stearate - 1.05 mg.

    Capsule body composition: ferric oxide yellow oxide - 0.0733%; titanium dioxide -1.0%; water - 14.50%; gelatin - up to 100%.

    Composition of cap capsule: ferric oxide black oxide - 0,0500%; titanium dioxide - 2.0%; water - 14.50%; gelatin - up to 100%.

    One 150 mg capsule contains:

    Active substance: tollerisone hydrochloride 150.00 mg;

    Excipients: cellulose microcrystalline - 70.00 mg; lactose monohydrate (sugar milk) - 43,50 mg; croscarmellose sodium - 12.00 mg; hypromellose - 3.00 mg; citric acid monohydrate - 4.50 mg; magnesium stearate - 2.00 mg.

    Capsule body composition: ferric oxide black oxide - 0,0500%; titanium dioxide - 2.0%; water - 14.50%; gelatin - up to 100%.

    Composition of cap capsule: dye quinoline yellow - 0.7500%; dye sunset sunset yellow - 0.0059%; titanium dioxide - 2.0000%; water - 14.50%; gelatin - up to 100%.

    Description:

    Dosage of 50 mg. Hard gelatin capsules № 2. Body, yellow and cream shade of color, the lid is light gray, opaque.

    Dosage of 150 mg. Capsules hard gelatinous № 0. The case is light gray, the porch is yellow, opaque.

    The contents of capsules are a mixture of powder and granules of white or almost white color with a characteristic odor. It is possible to compact the contents of the capsules into lumps in the shape of a capsule, which are easily disintegrated when pressed.

    Pharmacotherapeutic group:central muscle relaxant
    ATX: & nbsp

    M.03.B.X   Other muscle relaxants of central action

    M.03.B.X.04   Tolmoreyson

    Pharmacodynamics:

    Tolperisone is a central muscle relaxant. The mechanism of action is not fully understood. Tolmoreyson has a high affinity for the nerve tissue, reaching the highest concentrations in the brain stem, spinal cord and peripheral nervous system. The main effect of tolperisone is mediated by inhibition of spinal reflex arcs.Probably, this effect, together with the elimination of facilitating the excitation of descending pathways, provides the therapeutic effect of tolperisone.

    The chemical structure of tolperisone is similar to that of lidocaine. Like lidocaine, it has a membrane-stabilizing action and reduces the electrical excitability of motor neurons and primary afferent fibers. Tolmoreyson dose-dependent brakes the activity of voltage-dependent sodium channels. Accordingly, the amplitude and frequency of the action potential decreases. The depressing effect on the potential-dependent calcium channels was proved. It is assumed that, in addition to its membrane-stabilizing action tolperisone can also inhibit the release of the mediator.

    Tolmoreyson has some weak properties of α-adrenergic antagonists and antimuscarinic action.

    Pharmacokinetics:

    After oral administration tolperisone well absorbed in the small intestine. The maximum plasma concentration is noted after 0.5-1 h after administration. Due to expressed pre-systemic metabolism, bioavailability is about 20%.Fat-rich foods increase the bioavailability of the ingested tolperisone to about 100% and increase the maximum plasma concentration by about 45% compared with the administration of the drug on an empty stomach, delaying the time to reach a maximum concentration of about 30 minutes. Tolmoreyson intensively metabolized in the liver and kidneys. The compound is almost completely (more than 99%) excreted by the kidneys in the form of metabolites. Pharmacological activity of metabolites is unknown. Half-life after oral administration - about 2.5 h.

    Indications:Symptomatic treatment of spasticity in adults due to stroke.
    Contraindications:

    - Hypersensitivity to any of the components of the drug;

    - Myasthenia gravis gravis;

    - Children's age under 18 years;

    - breast-feeding;

    - lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

    Pregnancy and lactation:

    Pregnancy

    In experimental studies on animals, teratogenic effects of tolperisone were not detected. Due to the lack of meaningful clinical data tolperisone should not be used during pregnancy (especially in the first trimester), except when the expected benefit definitely justifies the potential risk to the fetus.

    Breastfeeding period

    Since there is no data on the isolation of tolperisone with breast milk, its use during the period of breastfeeding is contraindicated.

    Dosing and Administration:

    Inside, after eating, without chewing, without opening the capsule, squeezed a little water. Bioavailability of tolperisone decreases with fasting.

    The dose of the drug is selected based on the individual needs of the patient and the tolerability of the drug.

    50 mg 3 times a day, gradually increasing the dose to 150 mg 3 times a day.

    The recommended daily dose is 150-450 mg, divided into 3 parts.

    Patients with renal insufficiency

    The experience of using tolperisone in patients with renal insufficiency is limited, in this category of patients there were more often undesirable reactions. Therefore, in patients with impaired renal function of a moderate degree, a dose of tolperisone should be selected, with careful monitoring of the patient's health and control of kidney function. The use of the drug is not recommended in patients with severe renal failure.

    Patients with hepatic insufficiency

    Experience with the application of tolperisone in patients with hepatic insufficiency is limited, in this category of patients more often there were undesirable reactions.Therefore, in patients with impaired liver function of a moderate degree, a dose of tolperisone should be selected, with careful monitoring of the patient's health and control of liver function. The use of the drug is not recommended in patients with severe hepatic insufficiency.

    Side effects:

    The safety profile of tolperisone drugs is supported by data from more than 12,000 patients. According to these data, the most frequent violations are from the skin and subcutaneous tissues, general, neurological and gastrointestinal disorders.

    During the post-registration period, the number of reports received about the development of hypersensitivity reactions associated with the application of tolperisone was about 50-60% of all received messages. In most cases, these were not serious adverse reactions. Allergy-threatening reactions have been reported very rarely.

    The incidence of adverse reactions is classified according to the recommendations of the World Health Organization, is characterized as: very often (≥1 / 10), often (≥1 / 100, <1/10), infrequently (≥1 / 1000, <1/100), rarely (≥1 / 10000.<1/1000), very rarely (<1/10000), including single cases, the frequency is unknown (can not be calculated on the basis of available data).

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

    From the immune system; rarely - hypersensitivity reactions *, anaphylactic reactions; very rarely - anaphylactic shock.

    From the side of metabolism and nutrition: infrequently - anorexia, a very rare polydipsia.

    From the side of the psyche: infrequently - sleep disturbance, insomnia; rarely - weakness, depression; very rarely confusion.

    From the nervous system: infrequently - headache, dizziness, drowsiness; rarely - attention deficit disorder, tremor, convulsions, paresthesia, malaise, lethargy.

    From the side of the organ of vision: rarely - reduced visual acuity.

    From the side of the hearing organ: rarely - noise in the ears, vertigo.

    From the cardiovascular system: infrequently - arterial hypotension; rarely - angina pectoris, tachycardia, palpitation, "tides" of blood to the face; very rarely - a bradycardia.

    From the respiratory system: rarely shortness of breath, nasal bleeding, tachypnea.

    From the gastrointestinal tract: infrequently - discomfort in the abdomen, dyspepsia, diarrhea, dry mouth, nausea; rarely - epigastric pain, constipation, flatulence, vomiting.

    From the liver and biliary tract: rarely - moderate hepatic insufficiency.

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

    From the musculoskeletal system and connective tissue: infrequently - muscle pain, muscle weakness, pain in the limbs; rarely - discomfort in the limbs; very rarely - osteopenia.

    From the side of the kidneys and urinary tract: rarely - enuresis, proteinuria.

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

    Laboratory indicators: rarely - hyperbilirubinemia, impaired liver function, thrombocytopenia, leukocytosis; very rarely hypercreatininaemia.

    * Post-event monitoring reported angioedema, including facial edema and lips (frequency unknown).
    Overdose:

    Data on overdose of tolperisone are few.

    In preclinical studies of acute toxicity, high doses of tolperisone caused ataxia, tonic-clonic convulsions, dyspnea and respiratory paralysis.

    Tolperisone does not have a specific antidote. In case of an overdose, symptomatic and supportive treatment is recommended.

    Interaction:

    Studies of pharmacokinetic drug interaction with a marker substrate of isoenzyme CYP2D6 dextromethorphan showed that the simultaneous use of tolperisone can increase the blood levels of drugs that are metabolized predominantly by isoenzyme CYP2D6 (thioridazone, tolterodine, venlafaxine, atomoxetine, desipramine, dextromethorphan, metoprolol, nebivolol, perphenazine ).

    In laboratory experiments on human liver microsomes and human hepatocytes, significant inhibition or induction of other isoenzymes CYP (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP1A2, CYP3A4) it is not revealed.

    In connection with the variety of metabolic pathways of tolperisone, an increase in the exposure of tolperisone with the simultaneous use of isoenzyme substrates CYP2D6 and (or) otherx preparations are not expected.

    Bioavailability of tolperisone decreases with fasting.

    Although tolperisone is a drug of central action, its sedative effect is very low. When combined with other central muscle relaxants, the dose of tolperisone should be reduced.

    Tol- perisone enhances the action of niflumic acid, therefore, with simultaneous use, a reduction in the dose of niflumic acid or other non-steroidal anti-inflammatory drugs (NSAIDs) should be considered.

    Special instructions:

    The most frequent adverse reactions are hypersensitivity reactions.

    Allergic reactions are manifested from mild to severe to systemic, including anaphylactic shock. Symptoms of allergic reactions: redness, rash, hives, itching, angioedema (Quincke's edema), tachycardia, arterial hypotension and dyspnea.

    Female patients with hypersensitivity reactions to other drugs or allergic reactions in the anamnesis are at higher risk.

    In the case of a known hypersensitivity to lidocaine with tolperisone, caution should be exercised due to possible cross-reactions.

    Patients should be careful about any symptoms of hypersensitivity. If symptoms occur, stop taking tolperisone immediately and consult a doctor immediately. Do not reassign tolperisone after an episode of hypersensitivity to the drug containing it.

    Effect on the ability to drive transp. cf. and fur:

    Tolperisone does not affect the ability to drive vehicles and mechanisms. Patients who experience dizziness, drowsiness, attention disturbances, cramps, visual impairment, or muscle weakness while taking the drug should consult a doctor.

    Form release / dosage:

    Capsules, 50 and 150 mg.

    Packaging:

    By 5, 7, 10, 20, 30 capsules in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

    For 10, 20, 30, 40, 50, 60 or 100 capsules in cans of polyethylene terephthalate or cans of polymeric for medicines.

    One jar or 1, 2, 3, 4, 5, 6 or 10 contour squares, together with the instructions for use, are placed in a cardboard package (bundle).

    It is allowed to bundle 2 or 3 cardboard packages (packs) into a group package (shipping container) made of cardboardfor consumer packaging.

    Storage conditions:

    In the dark place at a temperature of no higher than 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    Do not use after the expiry date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003217
    Date of registration:23.09.2015
    Expiration Date:23.09.2020
    The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia
    Manufacturer: & nbsp
    Representation: & nbspOZONE LLC OZONE LLC Russia
    Information update date: & nbsp26.07.2016
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