Composition
Active ingredient: Tolperisone hydrochloride, in the composition of 1 tablet-50 or 150 mg. Additional ingredients (for 50/150 mg tablets): auxiliary substances: 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 (milk sugar) (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 action
Tolperisone is a centrally acting muscle relaxant whose mechanism of action is not fully understood. It is known that the drug has a high affinity (binding strength) to nervous tissue, reaches the highest concentrations in the brain stem, in the peripheral nervous system and spinal cord. The main effect of Tolperisone is associated with the inhibition of spinal reflex arcs, which, along with eliminating the facilitation of arousal 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 potential-dependent sodium channels, which reduces the frequency and amplitude of the action potential. Tolperisone was found to have a depressing effect on potential-dependent calcium channels. It has an antimuscarinic effect and some weakly expressed properties of alpha-adrenergic antagonists. It is assumed that it can also inhibit the release of mediators.
Indications
According to the instructions, Tolperisone is used to treat stroke-related spasticity in adults. Also, the use of the drug is possible in the following cases: :
- extrapyramidal disorders (atherosclerotic and postencephalitic parkinsonism);
- cerebral and spinal paralysis (limb contracture, spinal automatism, hypertonus, muscle spasm);
- hypertonus in combination with other types of muscle tone disorders;Â
- the consequences of disorders of vascular innervation (intermittent angioneurotic dysbasia, acrocyanosis);
- diseases accompanied by muscle spasm, rigidity, dystonia;
- obliterating diseases of the arteries: obliterate. lifeless vessels of the extremities, Buerger’s disease (thromboangiitis obliterans), diabetic angiopathy, Raynaud’s syndrome;
- infantile spastic paralysis (little’s disease);
- encephalopathy vascular Genesis;
- epilepsy;
- post-thrombotic disorders of lymphatic and venous blood circulation, trophic ulcers of the lower leg.
Recommendations for use
Tolperisone tablets should be taken orally after a meal: swallow whole, without breaking or chewing, and drink a sufficient amount of water. When taking the drug 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, while maintaining three times a day.
Contraindications
- age up to 18 years;
- glucose-galactose malabsorption, lactase deficiency, lactose intolerance;
- myasthenia gravis;
- breastfeeding;
- hypersensitivity to any of the components of the drug.
Side effects
According to data from clinical use of the drug in more than 12,000 patients, general disorders, gastrointestinal and neurological phenomena, as well as skin and subcutaneous tissue disorders are most often noted. The development of hypersensitivity reactions was reported in the post-marketing period, their number was 50-60% of all 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 Tolperisone therapy are classified as follows: very common – ≥ 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 – Tolperisone can cause the following disorders on the part of various organs and systems of the body:
- nervous system: infrequently – drowsiness, headache, dizziness; rarely – paresthesia, malaise, seizures, tremor, attention deficit disorder, epilepsy, lethargy;
- psyche: often – insomnia, insomnia; rarely – depression, feeling of weakness; rarely – confusion;
- metabolism: rarely – anorexia; very rarely – polydipsia;
- cardiovascular system: rarely – decreased blood pressure; rarely – palpitations, tachycardia, flushing to the face, angina; rarely – bradycardia;
- liver and biliary tract: rarely – liver failure average degree;
- kidney and urinary tract: rarely – proteinuria, enuresis;
- respiratory system: rarely – nosebleeds, shortness of breath, tachypnea;
- blood and lymphatic system: rarely – lymphadenopathy, anemia;
- gastrointestinal tract: rarely – dry mouth, abdominal discomfort, diarrhea, nausea, dyspepsia; rarely – flatulence, constipation, epigastric pain, vomiting;Â
- musculoskeletal system and connective tissue: often – pain in the limbs, weakness and muscle pain; rarely – a feeling of discomfort in the extremities; very rarely – osteopenia;
- immune system: rarely – anaphylactic and hypersensitivity reactions (angioedema, including lips, and face); very rarely – anaphylactic shock;
- skin and subcutaneous tissue: rarely – rash, skin rash, allergic dermatitis, urticaria, pruritus;Â
- organs of hearing and of vision: rarely – tinnitus, vertigo, decreased visual acuity;
- laboratory tests: rarely – leukocytosis, thrombocytopenia, hyperbilirubinemia, hepatic impairment; rarely – gipercreatininemia;
- other: rarely – malaise, fatigue, asthenia; rarely – thirst, a feeling of heat, irritability, feeling of intoxication; very rarely – discomfort in the chest.
Interaction
Tolperisone, when used concomitantly, can increase the blood content of drugs that are mainly metabolized with the participation of the CYP2D6 isoenzyme, 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, and CYP3A4) was detected in laboratory experiments. The bioavailability of tolperisone decreases when taken on an empty stomach. Tolperisone enhances the effects of nonsteroidal anti-inflammatory drugs, including niflumic acid, so when they are co-administered, dose adjustment may be required. With the simultaneous use of other central muscle relaxants, the dose of Tolperisone should be reduced. When combined with CYP2D6 substrates and/or other drugs, tolperisone exposure is not expected to increase.
Overdose
There are few reports of overdose cases. Tonic-clonic seizures, ataxia, dyspnea, and respiratory paralysis have been reported in preclinical studies of Tolperisone acute toxicity at high doses. There is no specific antidote. Treatment in case of overdose is carried out symptomatic and supportive.
Special instructions
Frequent side effects of the drug are hypersensitivity reactions, which can occur from mild skin to severe systemic, including anaphylactic shock. Symptoms of an allergic reaction include rash, redness, itching, urticaria, angioedema, shortness of breath, hypotension, and tachycardia. Women who have a history of allergic or hypersensitivity reactions to other medications are at a higher risk. Special care should be taken in cases of known hypersensitivity to lidocaine, as cross-reactions may occur. Patients should be warned to be alert to the occurrence of any possible symptoms of hypersensitivity. If they develop, you should immediately cancel the drug and consult a doctor. After an episode of hypersensitivity, repeated use of Tolperisone is prohibited.
Storage conditions
A place protected from light and inaccessible to children, with a temperature of up to 25 °C.
Shelf
life is 3 years.
Active ingredient
Tolperizon
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
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