Symptomatic treatment of muscle spasm in adults after a stroke.
active substance: tolperisone;
1 tablet contains tolperisone hydrochloride 150 mg;
excipients: microcrystalline cellulose; lactose monohydrate; stearic acid; potato starch; corn starch; talc; citric acid, monohydrate; colloidal anhydrous silica; hypromellose; titanium dioxide (E 171); polyethylene glycol 6000.
Main physical and chemical properties: film-coated tablets, white or almost white, round with a biconvex surface.
Tolperisone is a centrally acting muscle relaxant. The mechanism of action of tolperisone is not fully understood.
It has a high affinity for nervous tissue, reaching the highest concentrations in the brain stem, spinal cord and peripheral nervous system.
The most significant effect of tolperisone is its inhibitory effect on the spinal reflex pathway. Probably, this effect together with the inhibitory effect on the descending conduction pathways determines the therapeutic benefit of tolperisone.
The chemical structure of tolperisone is similar to the structure of lidocaine. Like lidocaine, it has a membrane-stabilizing effect and reduces the electrical excitability of motor neurons and primary afferent fibers. Tolperisone dose-dependently inhibits the activity of potential-dependent sodium channels. Accordingly, the amplitude and frequency of the action potential decreases.
The inhibitory effect on potential-dependent calcium channels has been proven. It is assumed that in addition to its membrane-stabilizing action, tolperisone may also inhibit the release of the mediator.
To top it all off, tolperisone has some weakly pronounced properties of α-adrenergic antagonists and has an antimuscarinic effect.
Clinical efficacy and safety. Tolperisone has been shown to be effective in treating muscle spasms after a stroke. It is known that during treatment with tolperisone there was a highly significant reduction in spasticity.
There is evidence that with brain damage, the efficacy of tolperisone in the Barthel index was comparable to that of baclofen.
Data on the efficacy of tolperisone in increased muscle tone in patients with musculoskeletal disorders other than post-stroke muscle spasm are conflicting. Some studies have shown positive results for some tests, while other studies have not shown the benefits of tolperisone in such diseases.
Symptomatic treatment of muscle spasm in adults after stroke.
- Hypersensitivity to the active substance or to chemically similar eperisone, or to any of the excipients.
- Myasthenia gravis.
- Breastfeeding period.
Method of application and dosage
The drug should be taken after a meal, washed down with a glass of water. Insufficient food intake may reduce the bioavailability of tolperisone.
Adults, depending on individual needs and tolerability – 150-450 mg / day for 3 doses.
The duration of treatment is determined individually.
Patients with impaired renal / hepatic function. Experience with tolperisone in patients with renal / hepatic impairment is limited, with a higher incidence of adverse events in such patients. Therefore, in moderate renal / hepatic impairment, individual dose titration with careful monitoring of the patient and monitoring of renal / hepatic function is recommended. Tolperisone is not recommended for severe renal / hepatic impairment.
Children. The safety and efficacy of tolperisone in children have not been studied.
Data on overdose are limited. Symptoms of overdose may mainly include drowsiness, gastrointestinal manifestations (nausea, vomiting, epigastric pain), tachycardia, hypertension, bradykinesia, and vertigo. In severe cases, there were reports of seizures and coma.
Treatment: symptomatic and supportive therapy. There is no specific antidote.
- From the blood and lymphatic system: anemia, lymphadenopathy.
- From the immune system: hypersensitivity reaction, anaphylactic reaction, anaphylactic shock.
- From the nervous system: headache, dizziness, drowsiness, attention deficit, tremor, convulsions, hypoesthesia, paresthesia, sleep disturbances, confusion, lethargy (increased drowsiness), insomnia, decreased activity, depression.
- From the senses: visual disturbances, tinnitus, vertigo.
- From the vascular system: hypotension, skin redness.
- From the heart: angina, tachycardia, tachycardia, low blood pressure, bradycardia.
- From the respiratory system: difficulty breathing, nosebleeds, rapid breathing.
- From the digestive system: nausea, vomiting, abdominal discomfort, diarrhea, dryness of the oral mucosa, dyspepsia, epigastric pain, constipation, flatulence, mild liver damage.
- On the skin: allergic dermatitis, hyperhidrosis, itching, urticaria, rash.
- From the musculoskeletal system: muscle weakness, myalgia, discomfort / pain in the extremities, osteopenia.
- From the urinary system: enuresis, proteinuria.
- Common disorders: asthenia, discomfort, fatigue, polydipsia, anorexia, intoxication, fever, irritability, thirst, chest discomfort.
- Laboratory indicators: increase in the concentration of bilirubin in the blood, change in the activity of liver enzymes, decrease in the number of platelets, leukocytosis, increase in the concentration of creatinine in the blood.
In the original packaging at a temperature not exceeding 25 oC.
Keep out of reach of children.