Tolizor
Tolizor: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Tolizor
ATX code: M03BX04
Active ingredient: tolperisone (tolperisone)
Manufacturer: LLC "Ozon" (Russia)
Description and photo updated: 20.11.2018
Prices in pharmacies: from 170 rubles.
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Tolizor is a centrally acting muscle relaxant.
Release form and composition
Tolizor is available in the form of hard gelatinous opaque capsules:
- 50 mg: size No. 2, with a yellow-cream body and a light gray lid;
- 150 mg: size no. 0, with a light yellow body and a yellow cap.
The contents of the capsules are a mixture of granules and powder (there may be seals in the form of lumps in the shape of a capsule, which are easily destroyed when pressed) of almost white or white color with a characteristic odor.
Packing of capsules: 10, 20, 30, 40, 50, 60 and 100 pcs. in banks, in a cardboard box 1 can; 5, 7, 10, 20 and 30 pcs. in blisters, in a cardboard box 1, 2, 3, 4, 5, 6 or 10 packages. A complete set of 2 and 3 cardboard packs in a group package (shipping container) is possible.
Composition of 1 capsule Tolizor:
- active substance: tolperisone hydrochloride - 50 or 150 mg;
- auxiliary components (capsules 50/150 mg): microcrystalline cellulose (55.22 / 70 mg), lactose monohydrate (milk sugar) (34.33 / 43.5 mg), croscarmellose sodium (6.32 / 12 mg), hypromellose (1.58 / 3 mg), citric acid monohydrate (1.5 / 4.5 mg), magnesium stearate (1.05 / 2 mg);
- body composition (capsules 50/150 mg): titanium dioxide (1/2%), water (14.5%), iron dye yellow oxide (0.0733 / 0.05%), gelatin (up to 100%);
- cap composition: 50 mg capsules - water (14.5%), titanium dioxide (2%), iron dye black oxide (0.05%), gelatin (up to 100%); capsules 150 mg - water (14.5%), titanium dioxide (2%), quinoline yellow dye (0.75%), sunset yellow dye (0.0059%), gelatin (up to 100%).
Pharmacological properties
Pharmacodynamics
Tolperisone - Tolizor's active ingredient is a centrally acting muscle relaxant. The mechanism of its action is not fully understood. The drug reaches the highest concentrations in the spinal cord, brain stem and peripheral nervous system. It has a high affinity for the nervous tissue. The main effect is associated with inhibition of the spinal reflex arcs. It is assumed that this effect of tolperisone against the background of eliminating the facilitation of the conduction of arousal along the descending pathways provides the therapeutic effect of Tolizor.
The chemical structure of tolperisone is similar to lidocaine. Like him, the drug has a membrane-stabilizing effect, reduces the electrical excitability of primary afferent fibers and motor neurons.
Depending on the dose, tolperisone inhibits the activity of voltage-gated sodium channels and, as a result, reduces the amplitude and frequency of the action potential.
It has been reliably established that the drug has a depressing effect on voltage-gated calcium channels. Presumably, tolperisone, in addition to providing a membrane-stabilizing effect, can also inhibit the release of a mediator.
In addition, tolperisone has an antimuscarinic effect and mild alpha-adrenergic antagonist properties.
Pharmacokinetics
Tolperisone after oral administration is well absorbed in the small intestine. The maximum concentration reaches after 30-60 minutes. It is characterized by low bioavailability - about 20%. Compared with taking the drug on an empty stomach, when eating food rich in fats, bioavailability increases to almost 100%, and also increases the maximum plasma concentration (by about 45%) and the time to reach the maximum concentration (by about 30 minutes).
Intensive metabolization of tolperisone occurs in the liver and kidneys. More than 99% of the dose is excreted by the kidneys in the form of metabolites, the pharmacological activity of which has not been established. The half-life is about 2.5 hours.
Indications for use
Tolizor is used for the symptomatic therapy of spasticity in stroke patients.
Contraindications
- myasthenia gravis;
- lactose intolerance, glucose-galactose malabsorption, lactase deficiency;
- age up to 18 years;
- lactation period;
- hypersensitivity to any of the Tolizor components.
Instructions for using Tolizor: method and dosage
Tolizor should be taken orally: swallow the capsules whole without opening or chewing, and drink plenty of water. It is advisable to take the drug after meals, since when taken on an empty stomach, its bioavailability decreases.
The doctor selects the optimal dose for each patient, depending on his needs and drug tolerance.
The initial recommended dose is 50 mg 3 times a day. If necessary, the dose is gradually increased, up to 150 mg 3 times a day.
The maximum daily dose of Tolizor is 450 mg in 3 divided doses.
The duration of therapy is individual.
Side effects
Tolizor is generally well tolerated, and its safety profile has been confirmed by experience in more than 12,000 patients.
In some cases, the following side effects occur:
- on the part of the psyche: infrequently (from ≥ 1/1000 to <1/100) - sleep disturbances, insomnia; rarely (from ≥ 1/10000 to <1/1000) - weakness, depression; very rarely (<1/10000) - confusion;
- from the nervous system: infrequently - drowsiness, dizziness, headache; rarely - malaise, tremor, paresthesia, convulsions, attention deficit disorder, lethargy;
- on the part of the hearing and visual organs: rarely - tinnitus, vertigo, decreased visual acuity;
- from the respiratory system: rarely - epistaxis, shortness of breath, tachypnea;
- on the part of the cardiovascular system: infrequently - arterial hypotension; rarely - flushing of the face, palpitations, tachycardia, angina pectoris; very rarely - bradycardia;
- from the gastrointestinal tract: infrequently - dry mouth, dyspepsia, abdominal discomfort, nausea, diarrhea; rarely - flatulence, epigastric pain, vomiting, constipation;
- on the part of the kidneys and urinary tract: rarely - proteinuria, enuresis;
- from the liver and biliary tract: rarely - moderate hepatic failure;
- from the side of metabolism and nutrition: infrequently - anorexia; very rarely - polydipsia;
- on the part of the musculoskeletal system and connective tissue: infrequently - muscle weakness, pain in the muscles and in the limbs; rarely - discomfort in the limbs; very rarely - osteopenia;
- from the immune system; rarely - hypersensitivity reactions (including angioedema, including the face and lips), anaphylactic reactions; very rarely - anaphylactic shock;
- on the part of the blood and lymphatic system: very rarely - lymphadenopathy, anemia;
- on the part of the skin and subcutaneous tissues: rarely - skin rashes, pruritus, urticaria, hyperhidrosis, allergic dermatitis;
- laboratory parameters: rarely - leukocytosis, hyperbilirubinemia, thrombocytopenia, liver dysfunction; very rarely - hypercreatininemia;
- others: infrequently - malaise, fatigue, asthenia; rarely - a feeling of warmth, thirst, irritability, a feeling of intoxication; very rarely - chest discomfort.
Overdose
Overdose data are insufficient to assess the degree of influence of tolperisone. In preclinical studies of acute toxicity when taking the drug in high doses, tonic-clonic seizures, ataxia, dyspnea, respiratory paralysis were noted. The specific antidote is unknown. Treatment of an overdose is symptomatic, including those aimed at maintaining the vital systems of the body.
special instructions
Allergic reactions to tolperisone can be of varying severity: from mild cutaneous to severe systemic, including anaphylactic shock. Allergy symptoms are redness, skin rashes, itching, urticaria, Quincke's edema, shortness of breath, arterial hypotension, tachycardia.
Compared to men, women who have a history of allergic reactions or hypersensitivity reactions to other drugs are more susceptible to hypersensitivity reactions.
Particular care should be taken in patients with known hypersensitivity to lidocaine, since cross-reactions may develop when using tolperisone.
Patients should be warned to seek immediate medical attention if they develop any symptoms of hypersensitivity. Even after one episode of hypersensitivity to tolperisone, its further use is contraindicated.
Influence on the ability to drive vehicles and complex mechanisms
Tolizor, as a rule, does not affect a person's attention, his motor and psychological functions. However, in some cases, it can cause drowsiness, blurred vision, dizziness, impaired attention, muscle weakness, convulsions. Such patients should see a doctor.
Application during pregnancy and lactation
The teratogenic effect of tolperisone in the course of experimental studies conducted on animals was not revealed. However, there are no significant clinical data, therefore, during pregnancy, especially in the first trimester, Tolizor is contraindicated, unless the intended benefit of therapy is definitely higher than the potential risks.
It is not known whether tolperisone is excreted in breast milk, therefore, the use of Tolizor is contraindicated during lactation.
Pediatric use
According to the instructions, Tolizor is not used to treat patients under the age of 18.
With impaired renal function
The experience of using the drug in patients with concomitant renal failure is limited, but it has been noted that side effects occur more often with this disease. In this regard, the use of Tolizor is not recommended in the presence of severe renal failure. In case of moderate renal impairment, careful dose selection, monitoring of the patient's condition and renal function are required.
For violations of liver function
The experience of using the drug in patients with concomitant hepatic insufficiency is limited, but it has been noted that side effects occur more often with this disease. In this regard, the use of Tolizor is not recommended in the presence of severe hepatic impairment. In case of moderate liver dysfunction, careful dose selection, monitoring of the patient's condition and liver function are required.
Drug interactions
When Tolizor capsules are taken on an empty stomach, the bioavailability of Tolperisone decreases.
In laboratory experiments on liver microsomes and human hepatocytes, no significant induction or inhibition of other CYP isoenzymes (CYP2C8, CYP1A2, CYP2C19, CYP2B6, CYP3A4, CYP2C9) was found.
If necessary, the simultaneous use of other central muscle relaxants should reduce the dose of Tolizor.
Tolperisone may increase the concentration in the blood of drugs metabolized primarily by the CYP2D6 isoenzyme, such as atomoxetine, nebivolol, dextromethorphan, venlafaxine, thioridazine, desipramine, tolterodine, metoprolol, perphenazine.
With the simultaneous use of substrates of the isoenzyme CYP2D6 and (or) other drugs, an increase in the exposure of tolperisone is not expected, which is explained by the diversity of its metabolic pathways.
Tolperisone enhances the effect of niflumic acid, therefore, with their combined use, a decrease in its dose may be required. The same goes for other non-steroidal anti-inflammatory drugs.
Analogs
Tolizor analogs are Tolperisone-OBL, Midocalm, Tolperisone.
Terms and conditions of storage
Store no more than 3 years at temperatures up to 25 ° C in a dark place out of reach of children.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tolizor
Reviews of Tolizor are mostly positive: the drug is effective, acts quickly, does not cause drowsiness, and is inexpensive.
Separately encountered negative reviews usually contain complaints about the development of side effects. Some patients write that the drug is not sold in all pharmacies.
Price for Tolizor in pharmacies
The price for Tolizor in a dosage of 150 mg is approximately 280–445 rubles. per pack of 30 capsules. The cost of the drug at a dosage of 50 mg is unknown, since at the moment it is not available commercially.
Tolizor: prices in online pharmacies
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Drug name Price Pharmacy |
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Tolizor 50 mg capsule 30 pcs. 170 RUB Buy |
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Tolizor 150 mg capsule 30 pcs. 210 RUB Buy |
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Tolizor 150 mg capsules combi-pack 1 + 1 30 pcs. 258 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
