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Active components of Tolperisonum the Hydrochloride and Lidocaine the Hydrochloride, and also excipients are a part of solution for injections Mydocalmum Richter:
- methylparahydroxybenzoate (E218 preservative);
- diethylene glycol ether monoethyl;
- water for injections.
Drug is issued in ampoules with a capacity of 1 ml in the form of solution for intravenous and intramuscular administration. One cardboard packaging contains the plastic pallet with 5 ampoules and the application instruction of solution for injections Mydocalmum.
Solution has an appearance transparent colourless (or slightly greenish) liquids with a characteristic specific smell.
Drug belongs to farmakoterapevtichesky group "Muscle Relaxants (Muscular Relaxants) with the Central Mechanism of Action" and is characterized by ability to render:
- membranostabiliziruyushchiya effects.
Pharmacodynamics and pharmacokinetics
The mechanism of effect of Tolperisonum solution which is a part is up to the end not studied. It is known that substance is characterized by high affinity (from armor. affinitas — "likeness") to nervous tissue. Its highest concentration are noted in a brain trunk, a spinal cord and PNS (peripheral nervous system).
Ability of Tolperisonum to have the braking effect on the reflex centers in a spinal cord is considered the most significant. It is probable that the similar effect in combination with the inhibiting impact on the efferent (descending) conduction paths defines therapeutic effect of Tolperisonum.
Tolperisonum possesses ability to prevent destruction of cellular membranes, and also reduces indicators of electric excitability of motor (motive) neurons and primary afferent shoots of the nervous cells which are carrying out sensitive impulses from various fabrics and bodies to CNS (central nervous system).
In addition, substance:
- reduces a threshold of painful sensitivity;
- blocks spinal and trunk monosinaptichesky and polisinaptichesky reflexes;
- selektivno reduces activity of caudal part of a complex of the nervous structures localized in the central departments of a tire of trunk part of a brain on all its extent (a so-called reticular formation of a trunk of a brain);
- reduces spasticity of muscles;
- reduces patholologically the raised muscles hyper tone;
- reduces muscular rigidity;
- reduces intensity of pain;
- facilitates any active movements and increases their amplitude;
- increases intensity of a peripheral blood-groove;
- has vasodilating effect;
- interferes with allocation of mediators in synapses (the similar effect develops, most likely, for the second time, owing to braking of processes of receipt of calcium ions (Ca2+) in the presynaptic (nervous) nerves).
Tolperisonum has weak spasmolytic effect and possesses properties of N-cholinolytic of the central action.
It is expressed in ability of substance to prevent or weaken mainly nicotinosimilar action of acetylcholine (the main neuromediator in a parasympathetic nervous system) and cholinomimetic means.
At the same time Tolperisonum does not make the expressed impact on peripheral parts of the nervous system.
Tolperisonum is characterized by good tolerance (in particular, it is well transferred by patients of old age), does not provoke development of cardiotoxic effects and disturbance of cognitive functions, is deprived of sedation.
The profile of safety of Tolperisonum is based on data of clinical trials in which patients with a muscle hyper tone of various etiology, and also on the basis of these spontaneous messages on any undesirable reactions took part.
During preclinical trials of pharmacological safety, toxicity level at course use, genotoxicity (ability to potentially provoke genovariations or development of tumors), ability to influence reproductive function of specific risks for patients it was not revealed.
Undesirable effects were noted only when the entered dose significantly exceeded the most admissible for the person. The last indicates the small importance for a clinical use.
Lidocaine works as local anesthetic and is characterized by ability dozozavisimo to brake activity of Na channels + (potential - dependent natrium channels) that, in turn, interferes with generation of impulses in the terminations of sensitive nerve fibrils and to carrying out impulses on them. And substance suppresses not only painful impulses, but also and impulses of other modalities.
At topical administration provokes vasodilatation, without having at the same time local irritative effect.
At a drug dosing Mydocalmum Richter according to the schemes provided in the application instruction, lidocaine has no systemic action on the patient's organism.
Tolperisonum the hydrochloride biotranformirutsya intensively in tissues of a liver and kidneys then it is almost completely brought out of an organism by kidneys in the form of metabolism products (more than 99% of the substance which came to an organism). There are no exact data on pharmacological activity of metabolites.
After administration of solution Mydocalmum in / in an elimination half-life of Tolperisonum of a hydrochloride makes an hour and a half.
Lidocaine a hydrochloride, getting to an organism, it is completely absorbed. And the speed of absorption depends on an injection site of drug and its dose. Time for which the maximum concentration of substance after an intramuscular injection is reached varies ranging from half an hour till 45 minutes.
Lidocaine contacts plasma proteins for 50-80%. Distribution of substance in various fabrics and bodies happens quickly enough.
Possesses ability to get through hematoencephalic (GEB) and plasma barriers and to be allocated with breast milk of the feeding woman. And concentration of lidocaine in milk makes 40% of concentration of substance in a blood plasma of mother.
Metabolization of lidocaine is carried out in liver tissues (approximately for 90-95%) under the influence of microsomal liver enzymes by means of dealkylation of an amino group and splitting of amide communication. As a result of this process active metabolites are allocated pharmacological.
From the patient's organism lidocaine is excreted together with bile (at the same time substance partially is exposed to a reabsorption in a digestive tract) and kidneys (to 10% of lidocaine it is removed in not changed look).
Indications to use
Indications to use Mydocalmum Richter:
- the hyper tone and spasticity of skeletal muscular tissue caused by organic lesions of TsNS (the had stroke, defeats of pyramidal system, injuries of a spinal cord of various etiology, multiple sclerosis, an inflammation of a head and spinal cord of a toksiko-allergic or virus etiology, etc.);
- the hyper tone and spasticity of skeletal muscular tissue caused by defeats of a musculoskeletal system (dystrophic processes of anatomical structures of a backbone, arthroses of large joints, a backbone spondylarthrosis, cervicobrachial neuralgia, a lumbar syndrome, etc.);
- the diseases which are followed by muscular dystonia;
- recovery therapy after operations (orthopedic, traumatologic, surgical).
In combination with other therapeutic actions Mydocalmum in ampoules is recommended:
- to patients for whom the pathologies connected with an obliteration of vessels (a diabetic angiopatiya, obliterating atherosclerosis, a diffusion scleroderma, Reynaud's syndrome, etc.) are diagnosed;
- to patients with the pathologies caused by frustration of an innervation of vessels (for example, a Crocq's disease).
Contraindications to appointment Mydocalmum Richter are:
- hypersensitivity to any of active or excipients, being a part of drug (including to the lidocaine and other amide drugs possessing mestnoanesteziruyushchy action);
- myasthenia in a severe form;
Also drug has age restrictions: pricks of medicine are contraindicated to the persons which did not reach 18-tiletny age.
Most often the organism of the patient reacts to Mydocalmum pricks a hyperemia of integuments in an injection site.
Such individual reactions as can infrequently be noted:
- frustration of a dream;
- headaches and dizzinesses, excessive drowsiness;
- arterial hypotension;
- dispeptic and dispepsichesky frustration;
- weakness and morbidity of muscles, extremity pains;
- symptoms of an asthenic syndrome, feeling of the general discomfort, increased fatigue.
To seldom arising side reactions which arise less than in one case from one thousand, but more often than time on ten thousand cases, belong:
- hypersensitivity reactions;
- depressions, decrease in physical activity;
- frustration of attention, spasm, excessive drowsiness, hypesthesia, tremor, etc.;
- visual disturbances;
- sonitus; the balance loss which is followed by feeling of rotation of own body around objects or on the contrary — rotation of objects around a body;
- tachycardia, stenocardia, decrease in indicators of arterial pressure;
- nasal bleeding, breath zatrudnennost, asthma;
- abdominal pains, locks, meteorism, vomiting;
- damages of a liver (usually benign);
- skin reactions (itch, burning, the strengthened sweating, emergence of rash, etc.);
- urine incontience, increase of concentration of protein in urine (over physiological norm);
- acrimony, strong thirst, emergence of feeling of intoxication;
- change of values of laboratory indicators (change of concentration of the bilirubin which is contained in blood, disturbance of activity of enzymes of a liver, etc.).
In isolated cases are possible:
- acute anaphylaxis;
- unnaturally strong, unquenchable thirst;
- confusion of consciousness;
- decrease in a cordial rhythm (to frequency less than 55 beats per minute);
- increase of concentration of the creatinine which is contained in blood.
Application instruction Mydocalmum Richter: route of administration and dosage of drug
According to the application instruction, pricks of Mydocalmum are shown only to patients 18 years are more senior. Solution is entered parenterally — into a vein or into a muscle.
Intramuscular injections assume introduction to the patient twice a day of the dose equal to 100 mg of Tolperisonum (contents of one ampoule).
In a vein once a day in the dose equal to 100 mg of Tolperisonum, very slowly is recommended to administer the drug.
How many days to prick Mydocalmum Richter, the attending physician depending on severity of a disease and the response of an organism of the patient to the appointed therapy defines.
Experience of treatment by drug of patients with the broken function of a liver and/or kidneys is limited. However in this group of patients the undesirable phenomena connected using Mydocalmum are noted more often than at patients with a healthy liver / kidneys.
For this reason for patients with moderately expressed damages of kidneys and/or a liver the optimum dose of drug is selected individually by a titration method. At the same time it is recommended to trace carefully a condition of the patient and all changes of function of livers/kidneys.
Tolperisonum is contraindicated to patients with severe forms of damage of a liver and/or kidneys.
The overdoses given about cases Mydocalmum are limited. Drug is characterized by a wide therapeutic index.
According to data of preclinical trials of acute toxicity of solution, at administration of drug in the doses significantly exceeding therapeutic such symptoms as are noted:
- disorders of coherence of movements of various muscles against absence at the patient of muscular weakness (ataxy);
- toniko-clonic convulsive attacks;
- breath zatrudnennost (up to its full stop).
The specific antidote for Tolperisonum is absent. When exceeding of the recommended dose the patient is recommended to make a gastric lavage. Further the symptomatic and supporting therapies are shown.
There are no data on research of compatibility of Mydocalmum therefore before introduction solution should not be mixed in one syringe with other medicines. The drug is administered separately from other drugs.
In spite of the fact that Mydocalmum Richter is characterized by ability to exert impact on TsNS, the probability of development of sedation at its use is absent. Appointment of drug in a combination to means of sedative action, sleeping pill, and also about means which part alcohol is is allowed.
Does not exert impact on effect of alcohol on TsNS.
In need of appointment Mydocalmum Richter in a combination with other muscular relaxants of the central action it is necessary to consider a question of decrease in a daily dose of Tolperisonum.
Tolperisonum potentsiirut pharmacological effect of niflumovy acid and other non-steroidal anti-inflammatory drugs because of what the dose of the last at a concomitant use them with Tolperisonum is recommended to be lowered.
Pharmacological effects of Tolperisonum strengthen the following drugs:
- means for the general anesthesia;
- muscular relaxants of peripheral action;
- psychotropic drugs;
Terms of sale
Drug belongs to the category of strong means and therefore it is released from drugstores only according to the recipe of the doctor.
It is necessary to store solution in original packaging in places, hardly accessible for children, observing temperature condition from 8 to 15 °C.
Period of validity
It is suitable for use within 3 years after date of production.
During treatment by the drug Mydocalmum Richter it is necessary to be careful at the driving and performance connected with risk for health and life of works, and also the works demanding the increased concentration of attention and high speed of psychomotor reactions.
Analogs Mydocalmum Richter
Analogs having pricked Mydocalmum Richter - it is the medicines having myorelaxation effect on an organism, but containing substances, other than active components of Mydocalmum, in the structure. Treat them:
- Liorezal Intratekalny;
PAY ATTENTION! Information on drugs on the website is help generalizing, collected from public sources and can form the basis for making decision on use of medicines it is not aware of treatment. Before medicine use Mydocalmum Richter surely consult with the attending physician.