Mydocalm solution for intravenous and intramuscular injection of 1 ml 5 pcs
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Active ingredients
Tolperisone
Release form
Solution
Composition
Active ingredient: tolperisone hydrochloride 100 mg, lidocaine hydrochloride 2. 5 mg. Excipients: methyl parahydroxybenzoate, diethylene glycol monoethyl ether, water dyne. Concentration of active ingredient (%): 10%
Pharmacological effect
Tolperisone is a centrally acting muscle relaxant. The exact mechanism of action of tolperisone is not fully understood. It has a high affinity for nervous tissue, reaching the highest concentrations in the brain stem, spinal cord, and peripheral nervous system. The main effect of tolperisone is associated with inhibition of spinal reflex arcs. It is likely that this effect, together with the obstacle to the initiation of downward pathway, provides the therapeutic effect of tolperisone: The chemical structure of tolperisone is similar to that of lidocaine. Like lidocaine, it has a stabilizing membrane effect and reduces the electrical excitability of motor neurons and primary afferent fibers. Tolperisone inhibits the activity of potential-dependent sodium channels in a dose-dependent manner. Accordingly, the amplitude and frequency of the action potential is reduced. A depressant effect has been proven on potential-dependent calcium channels. It is assumed that in addition to its membrane stabilizing effect, tolperisone may also inhibit the release of a mediator. To top it all, tolperisone has some weak alpha adrenergic antagonist properties and antimuscarinic effects.
Pharmacokinetics
Exposed to intensive metabolism in the liver and kidneys. Excreted by the kidneys, almost exclusively (> 99%) in the form of metabolites, the pharmacological activity of which is unknown. When administered intravenously, the half-life is ~ 1.5 h.
Indications
Treatment of pathologically increased tone and spasms of striated muscles arising from organic diseases of the central nervous system (including damage to the pyramidal tract, multiple sclerosis, stroke, myelopathy, encephalomyelitis), treatment of increased tone and muscle spasms, muscle contractures accompanying diseases of the movement organs (for example, spondylosis, spondyloarthrosis, cervical and lumbar syndromes, arthrosis of large joints),rehabilitation treatment after orthopedic and traumatologic operations, as part of combined therapy of vascular obliterans (obliterating atherosclerosis, diabetic angiopathy, thromboangiitis obliterans, Raynaud’s disease, diffuse scleroderma), diseases arising on the basis of vascular innervation disorder (acrocyanosis, intermittent angiopathy, intermittent angioplasty).
Contraindications
Severe myasthenia gravis, child age, pregnancy, lactation (breastfeeding), hypersensitivity to the components of the drug, including to lidocaine. With caution should use the drug for renal and hepatic failure. Dose adjustment is not required.
Precautionary measures
Apply strictly on doctor's prescription to avoid complications. Mydocalm does not affect the ability to drive and to perform work associated with increased risk.
Use during pregnancy and lactation
According to preclinical studies, tolperisone does not have a teratogenic effect. In the absence of clinical studies, the prescription of Mydocalm during pregnancy, especially in the first trimester, is possible only if the expected benefit clearly exceeds the risk of harm to the fetus. The use of tolperisone during lactation is contraindicated due to the lack of relevant data on the penetration of tolperisone into breast milk.
Dosage and administration
Adults are given daily intramuscular administration of 100 mg 2 times a day, or cc 100 mg 1 per day.
Side effects
On the part of the digestive system: nausea, vomiting, feeling of discomfort in the stomach. From the side of the central nervous system: muscle weakness, headache. Since the cardiovascular system: arterial hypotension. Allergic reactions: rarely - skin rash, pruritus, erythema, urticaria, angioedema, anaphylactic shock, shortness of breath.
Overdose
Data overdose Mydocalm few. Mydocalm has a wide therapeutic interval, describes the cases of children ingestion of 600 mg of the drug, proceeding without any special serious toxic symptoms. In some cases, children experienced minor adverse reactions after ingestion of 300-600 mg daily doses of the drug.In preclinical studies of acute toxicity, high doses caused ataxia, tonic-clonic convulsions, dyspnea, and respiratory paralysis. Mydocalm does not have a specific antidote. In case of overdose, symptomatic and supportive treatment is recommended.
Interaction with other drugs
Studies Pharmacokinetic drug interactions with the marker CYP2D6 substrate dextromethorphan has shown that the simultaneous use of tolperisone can raise blood levels of drugs that are metabolized mainly CYP2D6 (tioridazon, tolterodine, venlafaxine, atomoxetine, desipramine, dextromethorphan, metoprolol, nebivalol, perphenazine). Laboratory experiments on human liver microsomes and human hepatocytes showed no significant inhibition or induction of other CYP isoenzymes (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP1A2, CYP3A4). There is no intention to increase the effects of tolperisone with simultaneous use of CYP2D6 substrates and / or other drugs due to the variety of tolperisone metabolic pathways. Although tolperisone is a centrally acting drug, its sedative effect is very low, so it can be administered in combination with sedatives, hypnotic drugs and tranquilizers. In the case of simultaneous administration with other centrally acting muscle relaxants, the dose of tolperisone should be reduced. Tolperisone has no effect on the effect of alcohol on the central nervous system. Tolperisone enhances the action of niflumic acid, therefore, with simultaneous use, the possibility of reducing the dose of niflumic acid or other NSAIDs should be considered.
special instructions
The drug is not used in children. Hypersensitivity Reactions: During the post-registration period, the most frequently reported development of hypersensitivity reactions. Allergic reactions ranged from mild skin reactions to severe systemic reactions, including anaphylactic shock. Symptoms of an allergic reaction: erythema, rash, urticaria, pruritus, angioedema (angioedema), tachycardia, hypotension and shortness of breath. Patients with a history of hypersensitivity to other drugs or allergic reactions in history are at higher risk.In the case of known hypersensitivity to lidocaine, extreme caution should be exercised during the use of tolperisone due to possible cross-reactions. Patients should be advised to be attentive to any symptoms of hypersensitivity. If symptoms develop, stop using tolperisone immediately and consult a doctor immediately. Do not reapply tolperisone after an episode of hypersensitivity to tolperisone. Influence on ability to drive vehicles and work with mechanisms. Mydocalm does not affect the ability to drive vehicles and work with mechanisms. Patients who have experienced dizziness, drowsiness, impaired attention, convulsions, visual impairment or muscle weakness during the use of the drug should consult a doctor!