Tolperisone
Tolperisone: 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: Tolperisone
ATX code: M03BX04
Active ingredient: Tolperisone (Tolperisone)
Producer: ATOLL LLC (Russia)
Description and photo update: 2018-27-11
Prices in pharmacies: from 149 rubles.
Buy
Tolperisone is a centrally acting muscle relaxant.
Release form and composition
The dosage form of Tolperisone is film-coated tablets: round, biconvex, almost white or white, with a characteristic odor (in blisters of 7, 10, 14, 20, 25 and 30 pcs., In a cardboard box 1, 2, 3, 4, 5 or 10 packs; 5, 10, 20, 30, 40, 50 and 100 pcs. In polyethylene terephthalate or polypropylene cans, in a cardboard box 1 can).
Active ingredient: tolperisone hydrochloride, in the composition of 1 tablet - 50 or 150 mg.
Additional components (for tablets 50/150 mg):
- excipients: microcrystalline cellulose (72.6 / 70 mg), croscarmellose sodium (7.6 / 12 mg), magnesium stearate (1.3 / 2 mg), hypromellose (1.9 / 3 mg), lactose monohydrate (sugar lactic) (45.1 / 43.5 mg), citric acid monohydrate (1.5 / 4.5 mg);
- shell composition: macrogol-4000 (0.75 / 1.2 mg), hypromellose (3 / 4.8 mg), titanium dioxide (1.25 / 2 mg).
Pharmacological properties
Pharmacodynamics
Tolperisone is a centrally acting muscle relaxant, the mechanism of action of which is not fully understood. It is known that the drug has a high affinity (binding strength) to the nervous tissue, reaching the highest concentrations in the brain stem, in the peripheral nervous system and the spinal cord. The main effect of tolperisone is associated with the inhibition of the spinal reflex arcs, which, simultaneously with the elimination of the facilitation of the conduction of excitation along the descending pathways, presumably, determines the therapeutic property of tolperisone.
The chemical structure of the substance is similar to lidocaine, like it has a membrane-stabilizing effect, reduces the electrical excitability of primary afferent fibers and motor neurons.
The drug has a dose-dependent ability to inhibit the activity of voltage-gated sodium channels, as a result of which the frequency and amplitude of the action potential decreases.
It was found that tolperisone has a depressing effect on voltage-gated calcium channels. Possesses antimuscarinic action and some weakly expressed properties of alpha-adrenergic antagonists. It is assumed that it can also inhibit the release of neurotransmitters.
Pharmacokinetics
After oral administration, tolperisone is well absorbed in the small intestine. After about 30-60 minutes, the maximum plasma concentration is noted. Bioavailability is low - about 20% (due to pronounced first-pass metabolism). Compared with taking the drug on an empty stomach, a diet rich in fat increases the bioavailability of the drug to almost 100% and its maximum plasma concentration by about 45%, while delaying the time to reach peak concentration by an average of 30 minutes.
Tolperisone is metabolized in the kidneys and liver. It is excreted almost completely (at least 99%) in the form of metabolites by the kidneys. The pharmacological activity of metabolites has not been established.
The T ½ (half-life) period is about 2.5 hours.
Indications for use
According to the instructions, Tolperisone is used to treat spasticity due to stroke in adults.
Also, the use of the drug is possible in the following cases:
- extrapyramidal disorders (atherosclerotic and post-encephalitis parkinsonism);
- cerebral and spinal palsy (contracture of the limbs, spinal automatism, hypertonicity, muscle spasm);
- hypertonicity in combination with impaired muscle tone of another type;
- consequences of disorders of vascular innervation (intermittent angioneurotic dysbasia, acrocyanosis);
- diseases accompanied by muscle spasm, rigidity, dystonia;
- obliterating arterial diseases: obliterating atherosclerosis of the vessels of the extremities, Buerger's disease (thromboangiitis obliterans), diabetic angiopathy, Raynaud's syndrome;
- infantile spastic paralysis (Little's disease);
- encephalopathy of vascular origin;
- epilepsy;
- post-thrombotic disorders of lymph circulation and venous circulation, trophic ulcers.
Contraindications
- age up to 18 years;
- glucose-galactose malabsorption, lactase deficiency, lactose intolerance;
- myasthenia gravis;
- breast-feeding;
- hypersensitivity to any component of the drug.
Instructions for use Tolperisone: method and dosage
Tolperisone tablets should be taken orally after a meal: swallow whole without breaking or chewing, and drink plenty of water. When the drug is taken on an empty stomach, its bioavailability decreases.
The initial dose is 50 mg 3 times a day, then it is gradually increased to 150 mg, keeping three times a day.
Side effects
According to the data of clinical use of the drug in more than 12,000 patients, the most common disorders are general disorders, gastrointestinal and neurological phenomena, as well as disorders of the skin and subcutaneous tissues.
The development of hypersensitivity reactions were reported in the post-registration period, their number was 50-60% of all the data obtained. In the predominant case, non-serious side effects occurred. Severe, life-threatening allergic reactions have been reported very rarely.
According to the recommendations of the World Health Organization, side effects that occur during therapy with tolperisone are classified as follows: very often - ≥ 1/10, often - from ≥ 1/100 to <1/10, infrequently - from ≥ 1/1000 to < 1/100, rarely - from ≥ 1/10 000 to <1/1000, very rarely - <1/10 000, including isolated cases, unknown frequency - based on the available data, it is not possible to calculate the incidence of adverse reactions.
Tolperisone can cause the following disorders from various organs and body systems:
- nervous system: infrequently - drowsiness, headache, dizziness; rarely - paresthesia, malaise, convulsions, tremors, attention deficit disorder, epilepsy, lethargy;
- psyche: infrequently - sleep disturbances, insomnia; rarely - depression, feeling of weakness; very rarely - confusion of consciousness;
- metabolism: infrequently - anorexia; very rarely - polydipsia;
- cardiovascular system: infrequently - lowering blood pressure; rarely - a feeling of palpitations, tachycardia, flushing, angina pectoris; very rarely - bradycardia;
- liver and biliary tract: rarely - moderate hepatic failure;
- kidneys and urinary tract: rarely - proteinuria, enuresis;
- respiratory system: rarely - nosebleeds, shortness of breath, tachypnea;
- blood and lymphatic system: very rarely - lymphadenopathy, anemia;
- gastrointestinal tract: infrequently - dry mouth, abdominal discomfort, diarrhea, nausea, dyspepsia; rarely - flatulence, constipation, epigastric pain, vomiting;
- musculoskeletal system and connective tissue: infrequently - pain in the limbs, weakness and pain in the muscles; rarely - a feeling of discomfort in the limbs; very rarely - osteopenia;
- immune system: rarely - anaphylactic and hypersensitivity reactions (Quincke's edema, including lips and face); very rarely - anaphylactic shock;
- skin and subcutaneous tissues: rarely - hyperhidrosis, skin rash, allergic dermatitis, urticaria, pruritus;
- organs of hearing and vision: rarely - tinnitus, vertigo, decreased visual acuity;
- laboratory parameters: rarely - leukocytosis, thrombocytopenia, hyperbilirubinemia, liver dysfunction; very rarely - hypercreatininemia;
- others: infrequently - malaise, fatigue, asthenia; rarely - thirst, feeling of warmth, irritability, feeling of intoxication; very rarely - chest discomfort.
Overdose
There are few reports of overdose cases. In preclinical studies of acute toxicity of tolperisone, when taking high doses, tonic-clonic convulsions, ataxia, dyspnea and respiratory paralysis occurred.
There is no specific antidote. Treatment in case of overdose is symptomatic and supportive.
special instructions
Frequent side effects of the drug are hypersensitivity reactions, which can manifest from mild cutaneous to severe systemic, including anaphylactic shock. Symptoms of an allergic reaction are rash, redness, itching, urticaria, Quincke's edema, shortness of breath, arterial hypotension, tachycardia.
Women with a history of allergic or hypersensitivity reactions to other drugs are at a higher risk.
Increased caution should be exercised in the case of known hypersensitivity to lidocaine, since cross-reactions may develop.
Patients should be warned to be alert to any possible symptoms of hypersensitivity. If they develop, you should immediately cancel the drug and consult a doctor. After an episode of hypersensitivity, re-administration of tolperisone is prohibited.
Influence on the ability to drive vehicles and complex mechanisms
The negative effect of tolperisone on the reaction rate and attention was not noted. In case of muscle weakness, blurred vision or attention, drowsiness, seizures, consult a doctor.
Application during pregnancy and lactation
In the course of experimental studies carried out on animals, no teratogenic effect was revealed. But people have no experience of using tolperisone during pregnancy, and therefore, pregnant women, especially in the first trimester, are not prescribed the drug, except in cases of extreme necessity, when the expected benefit justifies the possible risks.
There is no data on the release of tolperisone with mother's milk, therefore, the drug is prohibited during lactation.
Pediatric use
Tolperisone tablets are not prescribed for children and adolescents under 18 years of age.
With impaired renal function
There is not enough experience with the use of the drug in patients with renal failure, however, it has been reliably established that side effects are more common in this category of patients, and therefore, Tolperisone is not prescribed for severe kidney damage. In case of moderate renal impairment, the dose should be carefully selected, and treatment should be carried out under the control of renal function and the general condition of the patient.
For violations of liver function
There is not enough experience with the use of the drug in patients with hepatic insufficiency, however, it has been reliably established that side effects are more common in this category of patients, and therefore Tolperisone is not prescribed for severe liver damage. In case of moderate hepatic dysfunction, the dose should be carefully selected, and treatment should be carried out under the control of liver function and the general condition of the patient.
Drug interactions
Tolperisone, with simultaneous use, can increase the blood content of drugs that are metabolized mainly with the participation of the isoenzyme CYP2D6, such as desipramine, venlafaxine, metoprolol, tolterodine, perphenazine, dextromethorphan, thioridazine, nebivolol, atomoxetine.
No significant induction or inhibition of other CYP isoenzymes (CYP1A2, CYP2C9, CYP2C8, CYP2C19, CYP2B6, CYP3A4) was found in laboratory experiments.
The bioavailability of tolperisone decreases when taken on an empty stomach.
Tolperisone enhances the effects of non-steroidal anti-inflammatory drugs, including niflumic acid, therefore, when they are combined, dose adjustment may be required.
With the simultaneous use of other centrally acting muscle relaxants, the dose of tolperisone should be reduced.
With the combined administration of substrates of the CYP2D6 isoenzyme and / or other drugs, an increase in the exposure of tolperisone is not expected.
Analogs
Tolperisone analogues are: Midocalm, Tolizor, Tolperisone-OBL.
Terms and conditions of storage
The shelf life is 3 years.
Storage conditions: place protected from light and out of reach of children, with temperatures up to 25 ° C.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews of Tolperisone
Reviews of Tolperisone from patients who took it are mostly positive. The drug is characterized by high efficiency, low cost and low incidence of side effects.
The price of Tolperisone in pharmacies
The price of Tolperisone averages 195 rubles per pack of 30 tablets at a dose of 50 mg and 260 rubles per pack of 30 tablets at a dose of 150 mg.
Tolperisone: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Tolperisone 50 mg film-coated tablets 30 pcs. 149 r Buy |
|
Tolperisone 150 mg film-coated tablets 30 pcs. RUB 218 Buy |
|
Tolperisone tablets p.p. 150mg 30 pcs. 255 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, 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!
