Description
Mydocalm Pharmacodynamics
Tolperizone is a myorelaxant of central action. The exact mechanism of action is not fully elucidated. Tolperizone has a high affinity to the nervous tissue, reaching the highest concentrations in the brainstem, spinal cord and peripheral nervous system. The main effect of tolperizone is mediated by inhibition of spinal reflex arcs. It is likely that this effect together with the elimination of facilitation of excitation conduction along the descending pathways provides the therapeutic effect of tolperizone.
The chemical structure of tolperizone is similar to that of lidocaine. Like lidocaine, it has a membrane stabilizing effect and reduces electrical excitability of motor neurons and primary afferent fibers. Tolperizone dose-dependently inhibits the activity of potential-dependent sodium channels. Consequently, the amplitude and frequency of the action potential decreases.
The inhibitory effect on potential-dependent calcium channels has been proved. It is assumed that in addition to its membrane-stabilizing effect, tolperizone may also inhibit mediator release. Tolperizone has some weak alpha-adrenergic antagonist properties and antimuscarinic action.
Indications
Symptomatic treatment of stroke-induced spasticity in adults. Treatment of painful muscle spasm associated with diseases of the musculoskeletal system (e.g., spondylosis, spondyloarthritis, cervical and lumbar syndromes, arthrosis of large joints).
Little’s disease (cerebral palsy in children) and other encephalopathies accompanied by muscular dystonia.
Contraindications
-Hypersensitivity to any of the components of the drug or chemically similar eperizone.
– Myasthenia gravis.
– Pregnancy and the period of breastfeeding.
– Childhood under 3 years of age.
– Galactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Dosage and administration
- Inside after a meal with a glass of water.
- Bioavailability of Tolperizone is reduced when taken on an empty stomach.
- The dose of the drug is chosen based on the individual patient’s needs and tolerance of the drug.
- Adults and adolescents over 14 years of age.
- Recommended daily dose is 150-450 mg divided into 3 intakes, depending on individual requirements and tolerability of the drug.
- Patients with renal insufficiency
Experience of tolperizone use in patients with renal insufficiency is limited, adverse reactions occurred more often in this category of patients. Therefore, in patients with moderate renal impairment the dose of tolperizone should be adjusted with close monitoring of the patient’s health status and renal function control. In patients with severe renal impairment, administration of tolperizone is not recommended. - Patients with hepatic impairment
Experience in the use of tolperizone in patients with hepatic impairment is limited; adverse reactions occurred more frequently in this category of patients. Therefore, in patients with moderate hepatic impairment, the dose of tolperisone should be adjusted with close monitoring of the patient’s health status and liver function monitoring. In severe liver damage the prescription of tolperizone is not recommended. - Administration in children
- Children from 3 to 6 years of age: the drug is prescribed orally in a daily dose of 5 mg/kg of body weight, divided into 3 doses.
- Children and adolescents 7 to 14 years of age: the drug is administered orally in a daily dose of 2-4 mg/kg distributed in 3 doses.
- Taking into account the small doses, children should be prescribed the drug in the form of film-coated tablets 50 mg.
