Instruction for use: Lidocaine + Tolperisone (Lidocainum + Tolperisonum)
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Pharmacological group
n Cholinolytics (muscle relaxants) in combination
Pharmacotherapy
Miorelaxant of central action. Has membrane stabilizing, local anesthetic effects. It inhibits impulses in primary afferent fibers and motor neurons, which leads to blocking of spinal mono- and polysynaptic reflexes. Probably, secondary inhibits the release of mediators by inhibition of the intake of Ca2 + in the synapses. In the brain stem eliminates the ease of carrying out excitation along the reticulospinal path. It enhances peripheral blood flow regardless of the influence of the central nervous system. In the development of this effect, the weak spasmolytic and alpha-adrenoblocking effects of tolperisone play a role.
Pharmacokinetics
It is well absorbed from the digestive tract. TCmax - 0,5-1 hours Bioavailability - 20%. Tolperisone is metabolized in the liver and kidneys. It is excreted by the kidneys in the form of metabolites (more than 99%). The pharmacological activity of metabolites is unknown. T1 / 2 after intravenous administration - 1.5 h.
Indication
Hypertonus and spasm of the striated musculature, arising from organic diseases of the central nervous system (including the defeat of pyramidal tracts, multiple sclerosis, stroke, myelopathy, encephalomyelitis), musculoskeletal system (including spondylosis, spondyloarthrosis, cervical and lumbar syndromes, Arthrosis of large joints). Restorative treatment after orthopedic and traumatological operations. In the combination therapy: obliterating vascular diseases (obliterating atherosclerosis, diabetic angiopathy, obliterating thromboangiitis, Raynaud's disease, diffuse scleroderma); Diseases arising from the disorder of vascular innervation (acrocyanosis, intermittent angioedema dysbasia).
Contraindications
Hypersensitivity (including lidocaine), myasthenia gravis, pregnancy, lactation period, children's age.
Dosing
In / m, slowly, adults - 100 mg (based on tolperisone) 2 times a day or 100 mg once a day.
Side effect
Muscle weakness, headache, decreased blood pressure, nausea, vomiting, a feeling of discomfort in the abdomen (with a decrease in the dose, side effects usually go away).
In rare cases - allergic reactions: skin rash (including erythematous, urticaria), skin itching, angioedema, anaphylactic shock, dyspnea).
Overdose
Symptoms: with oral intake of 300-600 mg of the drug in patients of childhood in some cases observed irritability. In animal experiments, large doses caused ataxia, tonic and clonic convulsions, dyspnoea and respiratory paralysis.
Treatment: there is no specific antidote, symptomatic and supportive treatment.
Interaction
Possible application in combination with sedative, hypnotic drugs and drugs containing ethanol (does not have an additional sedative effect).
Does not enhance the depriming effect of ethanol on the central nervous system.
Special instructions
During pregnancy and lactation, the drug can be used (especially in the first trimester of pregnancy) only if the expected benefit for the mother exceeds the increased risk for the fetus.
During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.