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

Excipients: cellulose microcrystalline - 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;

Shell composition: 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: 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;

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

Description:

Round, biconvex tablets, covered with a film coat 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:

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, 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,selection of dose tolperisone, with careful monitoring of the patient's health and control of kidney function. 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 tolperisone 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 received reports on 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 frequency 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 - sleep disturbance, 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 hearing organ: rarely - noise in the ears, vertigo.

From the side of 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, nosebleed, 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 impairment.

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: 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, no significant inhibition or induction of other CYP isoenzymes (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP1A2, CYP3A4) was detected.

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) other drugs is 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 an allergic reaction: redness, rash, hives, itching, angioedema (Quincke's edema), tachycardia, hypotension and shortness of breath.

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:

Tablets, film-coated, 50 and 150 mg.

Packaging:

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

For 5, 10, 20, 30, 40, 50 or 100 tablets in cans of polyethylene terephthalate for medicines,sealed with caps screwed on with a first opening control or by a "push-turn" system of polypropylene or polyethylene or polypropylene jars for drugs sealed with lids pulled with the control of the first opening from polyethylene or cans of polypropylene for drugs sealed with lids pulled with the control of the first opening from polyethylene high pressure.

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

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-003769

Date of registration:08.08.2016

Expiration Date:08.08.2021

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

Manufacturer: & nbsp

OZONE, LLC Russia

Representation: & nbspOZONE LLC OZONE LLC Russia

Information update date: & nbsp08.10.2016

Illustrated instructions

Instructions

Tolmoreyson (Tolperisone)