The drug reduces the tension of the striated muscles as a result of its action on the central nervous system. It has a high affinity for the nervous tissue, reaching the highest concentrations in the brainstem, spinal cord and peripheral nerve tissue. Tolperisone inhibits the reflex function of the spinal cord and the descending pathways of the spinal cord. It stabilizes the cell membrane and reduces the electrical excitability of motor neurons and sensory fibers. It has a dose-dependent inhibition on the voltage-dependent Calcium channels, and as a result reduces the amplitude and frequency of the action potentials. In addition to stabilizing the neuronal cell membrane, tolperisone may also reduce the release of relays. It also has weak antagonistic properties against α-adrenergic and muscarinic receptors. The drug is well absorbed from the gastrointestinal tract, the maximum plasma concentration reaches 0.5-1.5 hours. Due to the significant effect of the first pass, bioavailability is around 20%. It is metabolized in the liver and kidneys. It is excreted in the urine (> 99%) in the form of metabolites. T0,5 after oral administration is 2.5 hours.
Contraindications:
Hypersensitivity to tolperisone, eeperisone or any of the excipients. Myasthenia gravis. Breastfeeding period. Pregnancy (especially the first trimester) - relative contraindication.
Precautions:
Patients should be advised to be vigilant to detect any signs of hypersensitivity; if they occur, stop taking the medicine immediately. After the occurrence of a tolperisone hypersensitivity episode, it must not be used again. Women, patients with hypersensitivity to other medications or with a history of allergy may be at higher risk of hypersensitivity reactions. In the case of known hypersensitivity to Lidocaine, caution should be exercised when using tolperisone due to possible cross-reactions. Experience in patients with impaired renal or hepatic function is limited and a higher incidence of side effects has been observed in these patients. For moderate renal or hepatic dysfunction, individual titration is recommended, accompanied by close monitoring of the patient's condition and renal or hepatic function. Use in patients with severe renal or hepatic impairment is not recommended. Caution in elderly patients (increased risk of drowsiness and weakness); treatment should be started with small doses, carefully increased. The safety and efficacy of tolperisone in children has not been established. Due to the lactose content, the drug should not be used in patients with galactose intolerance, Lapp lactase deficiency or malabsorption of glucose-galactose.
Pregnancy and lactation:
Do not use during pregnancy (especially in the first trimester), unless the anticipated benefits to the mother outweigh the potential risk to the fetus. The drug is contraindicated during breastfeeding.
Side effects:
Uncommon: lack of appetite, sleep disturbance, insomnia, drowsiness, pain and dizziness, hypotension, abdominal discomfort, diarrhea, dry mouth, dyspepsia, nausea, muscular weakness, muscle pain, limb pain, weakness, feeling discomfort, fatigue. Rarely: hypersensitivity reaction, anaphylactic reaction, decreased activity, depression, attention disorders, tremor, epilepsy, hypesthesia, paresthesia, lethargy, blurred vision, tinnitus, dizziness, angina, tachycardia, palpitations, baked goods, dyspnea, bleeding from the nose, rapid breathing, abdominal pain, constipation, bloating, vomiting, mild liver damage, allergic skin reactions, excessive sweating, pruritus, urticaria, rash, inability to control urination and involuntary pricking, proteinuria,feelings of discomfort in the extremities, feeling hot, excitability, thirst, reduced blood pressure, increased bilirubin in the blood, changes in liver enzymes, reduced number of platelets, increased number of white blood cells. Very rare: anemia, enlarged lymph nodes, severe allergic reactions, polydipsia, confusion, bradycardia, osteopenia, discomfort in the chest, increased blood creatinine.
Dosage:
Orally. Adults: 150-450 mg daily in 3 divided doses. Table. should be taken after meals (to increase the bioavailability of tolperisone), with a glass of water.
(C)
