Tolperisone - instructions for use, doses, side effects, contraindications

Excipients: microcrystalline cellulose - 72.60 mg; lactose monohydrate (sugar milk) - 45.10 mg; croscarmellose sodium - 7.60 mg: hypromellose - 1.90 mg; citric acid monohydrate - 1.50 mg; magnesium stearate - 1.30 mg.

The composition of the shell: hypromellose - 3.00 mg, macrogol - 4000 - 0.75 mg, titanium dioxide - 1.25 mg.

One 150 mg tablet contains:

Active substance: tolperisone hydrochloride - 150.00 mg;

Excipients: microcrystalline cellulose - 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.

Sheath composition: hypromellose - 4.80 mg, macrogol - 4000 - 1.20 mg, titanium dioxide - 2.00 mg.

Description:

round biconvex tablets,Covered with a film shell of white or almost white, with a characteristic odor

Pharmacotherapeutic group:central muscle relaxant

ATX: & nbsp

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

M.03.B.X.04 Tolmoreyson

Pharmacodynamics:

Tolimerizon is a central muscle relaxant. The mechanism of action is not fully understood.Tolmoreyson has a high affinity for the nervous 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.A depressing effect on the potential-dependent calcium channels was demonstrated. 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 a-adrenergic antagonists and antimuscarinic action.

Pharmacokinetics:

Ingestion room 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 nights. The compound is almost completely (more than 99%) excreted by the kidneys in the form of metabolites. Pharmacological activity of metabolites is unknown. The half-life after oral administration is about 2.5 hours.

Indications:

Symptomatic treatment of tackiness in adults due to stroke.

Contraindications:

myasthenia gravis.

Children under 18 years old. Breast-feeding.

Hypersensitivity to any of the components of the drug

Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Pregnancy and lactation:In experimental studies on animals, the teratogenic effect of tolyserone has not been revealed. Due to the lack of significant clinical data, tolperisoy ns should be used during pregnancy (especially in the first trimester), unless the expected benefit clearly justifies the potential risk to the fetus.

Since data on the isolation of tolperisone with breast milk are not available, its use during the period of breastfeeding is contraindicated.

Dosing and Administration:

Inside, after eating, without chewing, not breaking the pill, squeezed a little water. Bioavailability of tolperisone decreases with fasting.

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

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 medium degree, it is necessary to select a dose of tolperisone. with careful monitoring of the patient's health and control of the function of the nights. In severe kidney damage, administration of tolperisone is not recommended.

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. In severe liver damage, administration of tolpirazone is not recommended.

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 messages received about the development of the reaction of type sensitivity.related to the application of tolperisone, was about 50-60% of all received messages. In most cases, these were non-serious end-point reactions. Allergy-threatening reactions have been reported very rarely.

The incidence of side effects 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 not known (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; very rarely - polydipsia. From the side of the psyche: infrequently - a violation of sleep. insomnia; rarely - weakness, depression; very rarely confusion.

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

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

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

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

From the respiratory system: rarely - shortness of breath, nosebleeds, tachypnea.

From the gastrointestinal tract: infrequently - discomfort, dyspepsia,

diarrhea, dry mouth, nausea: rarely-in the epigastrium, constipation, flatulence, vomiting.

From the side of the liver and bile ducts: rarely - moderate liver failure.

From the skin and subcutaneous tissues: rarely - allergic dermatitis, hyperhidrosis, skin itch, 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: infrequent - asthenia, fatigue, malaise; rarely a feeling of intoxication, a feeling of warmth, irritability, thirst; very rarely discomfort in the chest.

Laboratory indicators: rarely - giperbilirubinemia.violation of liver function, thrombocytopenia, leukocytosis; very rarely hypercreatininaemia.

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

Overdose:

Data on overdose of tolpernose are few.

In preclinical studies of acute toxicity, high doses of tolnzoia caused ataxia, gonico-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 the marker substrate of the CYP2D6 isoenzyme dextromethorphan have shown that concomitant use of tolnzoia can increase the blood levels of drugs that are metabolized predominantly by the isoenzyme CYP2D6 (thioridazone, tolgherodine. venlafaxine, atomoxetine, desipramia, dextromethorphan, metoprolol. nebivolol, perphenazine).

In laboratory experiments on human liver microsomes, no significant inhibition or induction of other CYP isoenzymes (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP1A2, CYP3A4) was detected.

Due to the diversity of the tolperisone metabolic pathways, an increase in the exposure of the dropsrizon with simultaneous application of the CYP2D6 isoenzyme substrates and (or) other NS preparations is expected.

Bioavailability of tolperisone decreases with fasting.

Despite the fact that tolperisop is a central-action drug, its sedative effect is very low. When combined with other muscle relaxants centrally acting dose tolperisone should be reduced.

Tolperizop iiflumovoy acid enhances the effect, however, while the application should consider a dose reduction iiflumovoy pesteroidnyh acid or other anti-inflammatory drugs (NSAIDs).

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 an allergic reaction: redness, rash,

urticaria, itching, angioedema (Quincke's edema), tachycardia, hypotension and shortness of breath.

Patients female Iola with hypersensitivity reactions to other medications 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 re-appoint tolperisope after a hypersensitivity episode 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:

Tablets, film-coated 50 and 150 mg.

Packaging:

By 7, 10, 14. 20, 25. 30 tablets in a contour mesh box made of a polyvinylchloride film and aluminum foil printed lacquered.

According to 5. 10, 20, 30, 40, 50 or 100 tablets in cans of poly-ethylene glycol or in polymeric cans for medicines.

One jar or one.2, 3, 4, 5 or 10 contour mesh packages together with the instruction but are placed in a cardboard package.

Storage conditions:

In the dark place at a temperature of ns above 25 ° C.

Keep away from 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-003131

Date of registration:10.08.2015

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZON PHARM, LLC Russia

Information update date: & nbsp14.09.2015

Illustrated instructions

Instructions

Tolmoreyson (Tolperisone)