Description
Tolperisone Pharmacodynamics
A myorelaxant of central action. The mechanism of action is not fully elucidated. Tolperizone has a high affinity to the nervous tissue, reaching the highest concentrations in the brain stem, 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, tolperizone 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. Accordingly, the amplitude and frequency of the action potential decreases. Inhibitory effects on potential-dependent calcium channels have also been shown. It is assumed that in addition to its membrane-stabilizing effect, tolperizone may also inhibit mediator release. Tolperizone has some weak properties of ?-adrenergic antagonists 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 tolperizone and/or other excipients of the drug;
– myasthenia gravis;
– children under 18 years of age;
– Breast-feeding period;
– lactose intolerance, lactase deficiency and/or glucose-galactose malabsorption.
Caution.
The drug should be used with caution in women, patients with hypersensitivity to lidocaine and/or other drugs or with allergy in anamnesis (see section “Special indications”), in patients with renal and hepatic insufficiency (see section “Dosage and administration”).
If you have any of the above mentioned conditions/diseases, consult your physician before taking this medicine.
Using during pregnancy and lactation
Pregnancy
Teratogenic action of tolperizone has not been revealed in experimental studies on animals. For the reason of lack of significant clinical data tolperizone should not be used during pregnancy (especially during the 1st trimester), except for cases when the expected benefits definitely justify the potential risk for the fetus.
Breastfeeding period
As there is no data on excretion of tolperizone with breast milk, its use during lactation is contraindicated.
Dosage and administration
- Orally, after a meal, without chewing, do not break the tablet, wash down with a small amount of water. The bioavailability of Tolperizone is reduced when taken on an empty stomach.
- At 50 mg 3 times a day, gradually increasing the dose to 150 mg 3 times a day.
- Patients with renal insufficiency
- Experience of tolperizone administration in patients with renal insufficiency is limited, adverse reactions occurred more often in this category of patients, therefore in patients with moderate renal dysfunction the tolperizone dose should be adjusted with careful monitoring of the patient’s health and renal function control. In severe renal impairment the 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 tolperizone should be adjusted with close monitoring of the patient’s health status and control of liver function. Administration of tolperizone is not recommended in severe hepatic impairment.
