Description
Tolizor 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-related spasticity in adults;
– Moderate to severe myofascial pain syndrome (including muscle spasm in dorsopathies).
Contraindications
Hypersensitivity to any of the components of the drug or chemically similar aperizone.
Myasthenia gravis.
Childhood under 18 years of age.
Breast-feeding.
Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Caution.
Use in women, patients with hypersensitivity to lidocaine and/or other drugs or who have a history of allergy (see section “Special considerations”) and patients with renal or hepatic impairment (see section “Administration and Dosage”).
If you have any of the above conditions / diseases, consult a physician before using the drug.
Dosage and administration
- Inside, after a meal, without chewing, do not open the capsule, wash down with a little 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.
- At 50 mg 3 times a day, gradually increasing the dose to 150 mg 3 times a day.
- The recommended daily dose is 150-450 mg divided into 3 parts.
- Patients with renal insufficiency
- The experience of using tolperizone in patients with renal impairment is limited; adverse reactions occurred more frequently in this category of patients. Therefore, in patients with moderate renal dysfunction it is necessary to adjust the dose of tolperizone with close monitoring of the patient’s health status and control of renal function. The use of the drug is not recommended in patients with severe renal insufficiency.
- Patients with hepatic impairment
- The experience of tolperizone use in patients with hepatic insufficiency is limited, adverse reactions occurred more often in this category of patients. Therefore, in patients with moderate liver dysfunction it is necessary to adjust the dose of tolperisone with close monitoring of the patient’s health status and control of liver function. The use of the drug is not recommended in patients with severe hepatic impairment.
