Tolpekain

General characteristics. Structure:

Active ingredients: 2,5 mg of lidocaine, 100 mg of Tolperisonum in 1 ml of solution.

Pharmacological properties:

Pharmacodynamics. Muscle relaxant of the central action. Has membrane stabilizing, mestnoanesteziruyushchy effects. Slows down carrying out impulses in primary afferent fibers and motor neurons that leads to blocking spinal mono - and polisinaptichesky reflexes. Possibly, for the second time slows down allocation of mediators by braking of receipt of Ca2 + in synapses. In a brainstem eliminates simplification of carrying out excitement on a reticulospinal way. Strengthens a peripheral blood stream irrespective of influence of TsNS. In development of this effect plays a role weak spasmolytic and alpha адреноблокируюший effects of Tolperisonum.

Pharmacokinetics. It is well soaked up from a GIT. TCmax  is 0,5–1 h. Bioavailability — 20%. Tolperisonum is metabolized in a liver and kidneys. It is allocated with kidneys in the form of metabolites (more than in 99%). Pharmacological activity of metabolites is unknown. T1/2  after intravenous administration is 1,5 h.

Indications to use:

The hyper tone and spasm of cross-striped muscles arising owing to organic diseases of TsNS (including defeat of pyramidal ways, multiple sclerosis, a stroke, a myelipathy, encephalomyelitis), a musculoskeletal system (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: obliterating diseases of vessels (obliterating atherosclerosis, diabetic angiopatiya, obliterating thromboangitis, Raynaud's disease, diffusion scleroderma); the diseases evolving from frustration of an innervation of vessels (a Crocq's disease, an intermittent angioneurotic dysbasia).

Route of administration and doses:

In oil, slowly, adult — 100 mg (counting on Tolperisonum) 2 times a day or on 100 mg of 1 times a day.

Features of use:

During pregnancy and a lactation drug can be used (especially in the I trimester of pregnancy) only if the expected advantage for mother exceeds the increased risk for a fruit.

During treatment it is necessary to be careful during the driving of motor transport and occupation other potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

Muscular weakness, headache, decrease in the ABP, nausea, vomiting, feeling of discomfort in a stomach (at reduction of a dose by-effects usually pass).

In rare instances — allergic reactions: skin rash (including erythematic, small tortoiseshell), skin itch, Quincke's disease, acute anaphylaxis, asthma).

Interaction with other medicines:

Use in a combination with sedative, the HP hypnotic drugs and drugs containing ethanol is possible (does not render additional sedation).

Does not strengthen the depriving of bonuses influence of ethanol on TsNS.

Contraindications:

Hypersensitivity (including to lidocaine), a myasthenia, pregnancy, the lactation period, children's age.

Overdose:

Symptoms: at oral administration of 300-600 mg of drug at patients of children's age in some cases observed irritability. In experiments on animals high doses caused an ataxy, tonic and clonic spasms, short wind and paralysis of breath.

Treatment: there is no specific antidote, the symptomatic and supporting treatment.

Storage conditions:

To store at a temperature of 2-8 °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:

Solution for injections of 100 mg of Tolperisonum + 2,5 mg of lidocaine, on 1 ml in each ampoule. On 5 or on 10 ampoules, together with the application instruction in cardboard packaging.