Tolperisonum

General characteristics. Structure:

Active ingredient: 50 mg or 150 mg of Tolperisonum in 1 tablet.

Pharmacological properties:

Pharmacodynamics. Possesses membrane stabilizing and mestnoanesteziruyushchy action, reduces painful sensitivity of peripheral nerve terminations, brakes conductivity of impulses in primary afferent and motive fibers that leads to blocking mono - and polisinaptichesky medullispinal reflexes. Possibly, for the second time, owing to braking of receipt of Ca2 + in presynaptic nerves, slows down allocation of mediators in synapses. Promotes braking of carrying out excitement on a reticulospinal way. Selectively reduces activity of a caudal part of a reticular formation of a brain, reducing spasticity. Reduces patholologically the raised muscle tone and muscle tension, reduces morbidity, facilitates any active movements. Has weak spasmolytic and adrenoceptor blocking effects, strengthens a peripheral blood stream irrespective of influence of TsNS.

It is well transferred by patients of late age, does not possess cardiotoxic action, it is deprived of sedation and does not worsen cognitive functions of patients.

Pharmacokinetics. At intake it is soaked up in a small intestine. Cmax in plasma is defined by 0,5–1 h. The effect of "the first passing" through a liver is expressed owing to what bioavailability makes about 20%. It is metabolized in a liver and kidneys. Pharmacological activity of metabolites is unknown. T1/2 is 1,5–2,5 h. It is removed by kidneys in the form of metabolites (more than 99%), less than 0,1% are removed by kidneys in not changed look during 24 h.

Indications to use:

Treatment patholologically the raised muscle tone and spasms of cross-striped muscles owing to organic diseases of TsNS (including defeat of pyramidal ways, multiple sclerosis, a stroke, a myelipathy, encephalomyelitis), and also accompanying musculoskeletal system diseases (including a spondylosis, a spondylarthrosis, cervical and lumbar syndromes, arthroses of large joints); recovery treatment after orthopedic and traumatologic operations; as a part of a combination therapy of obliterating diseases of vessels (obliterating atherosclerosis, a diabetic angiopatiya, an obliterating thromboangitis, Reynaud's syndrome), diseases evolving from frustration of an innervation of vessels (a Crocq's disease, an intermittent angioneurotic dysbasia). In pediatrics — Littl's disease (children's brain paralysis) and other encephalopathies which are followed by muscular dystonia.

Route of administration and doses:

Inside, the adult — usually since 50 mg 2–3 times a day, gradually raising a dose to 150 mg 2–3 times a day. To children from 1 year to 6 years — 5 mg/kg/days, detyam7-14 years — 2–4 mg/kg/days (in 3 receptions during the day).

Features of use:

Use at pregnancy and feeding by a breast. During pregnancy (especially in the I trimester) and during breastfeeding it can be applied only if the expected advantage for mother exceeds potential risk for a fruit.

The category of action on a fruit — is not determined by FDA.

Side effects:

From a nervous system and sense bodys: muscular weakness, headache, drowsiness.

From bodies of a GIT: nausea, vomiting, abdominal discomfort (usually pass at a dose decline).

Allergic reactions: acute anaphylaxis, bronchospasm, small tortoiseshell, erythema, skin itch.

Others: decrease in the ABP.

Interaction with other medicines:

The effect of Tolperisonum is strengthened by anesthetics, peripheral muscle relaxants, psychotropic drugs, a clonidine. It can be applied in a combination with sedative, the hypnagogues and drugs containing alcohol. Does not influence effect of alcohol on TsNS. Tolperisonum strengthens effect of niflumovy acid (at simultaneous use the dose decline of niflumovy acid can be required).

Contraindications:

Hypersensitivity, myasthenia, children's age till 1 year.

Overdose:

Data on overdose did not arrive. Has broad therapeutic range, in literature use of drug for children inside in a dose of 600 mg without manifestation of serious toxic symptoms is described. At intake of 300-600 mg of drug a day at children in some cases observed irritability.

At a research of acute peroral toxicity in experiments on animals high doses caused an ataxy, tonic and clonic spasms, short wind and paralysis of breath.

Possible symptoms: respiratory depression (at the expense of paresis of a diaphragm and direct inhibition of a respiratory center) and cordial activity, arterial hypotension.

Treatment: gastric lavage, symptomatic and maintenance therapy. There is no specific antidote.

Storage conditions:

To store at a temperature of 15-25 °C, in dry, protected from light and the place, unavailable to children. Period of validity 3 years. Not to use after the expiry date specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets of 50 mg. 20 tablets in each blister, on one, two or three blisters together with the application instruction in cardboard packaging.

Tablets of 150 mg. 10 tablets in each blister, on one, two or three blisters together with the application instruction in cardboard packaging.