Tolperizon-OBL

General characteristics. Structure:

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

Excipients: citric acid, lactoses monohydrate (sugar milk), hypro rod (hydroxypropyl cellulose), кросповидон, stearic acid.

Excipients for a cover: Опадрай II (Series 85) [polyvinyl alcohol, macrogoal (polyethyleneglycol), talc, titanium dioxide].

Pharmacological properties:

Pharmacodynamics. Muscle relaxant of the central mechanism of action. Has membrane stabilizing effect, slows down carrying out nervous impulses in primary afferent fibers and motor neurons that leads to blocking spinal mono - and polisinaptichesky reflexes. Possibly, mediates blocking of allocation of mediators by braking of receipt of Ca+2 in synapses. Slows down carrying out excitement on a reticulospinal way in a brainstem.

Irrespective of influence of the central nervous system strengthens a peripheral blood stream. In development of this effect the weak spasmolytic and anti-adrenergic effect of Tolperisonum can play a role.

Pharmacokinetics. After intake Tolperisonum is well soaked up from a small bowel. The maximum concentration in a blood plasma is reached in 30 min. - 1 h after reception, bioavailability because of the expressed presistemny metabolism makes about 20%.

Tolperisonum is extensively metabolized in a liver and kidneys. It is excreted with urine almost only (more than 99%) in the form of metabolites. Pharmacological activity of metabolites is unknown.

Indications to use:

Treatment patholologically the raised tone and spasms of cross-striped muscles caused by organic neurologic pathology (including defeat of pyramidal ways, multiple sclerosis, a stroke, a myelipathy, encephalomyelitis).

Treatment of the raised tone and muscular spasms, muscular contractures accompanying musculoskeletal system diseases (a spondylosis, a spondylarthrosis, arthrosis of large joints, cervical and lumbar pain syndromes).

Recovery treatment after operative measures in orthopedics and traumatology.

As a part of a combination therapy of obliterating diseases of vessels (obliterating atherosclerosis, a diabetic angiopatiya, an obliterating thromboangitis, a Raynaud's disease), and also diseases arising owing to disturbance of an innervation of vessels (a Crocq's disease, an intermittent angioneurotic dysbasia).

Route of administration and doses:

Inside. The adult an initial dose of 50 mg 2-3 times a day, with gradual increase up to 150 mg 2-3 times a day.

Duration of a course of treatment depends on weight and character of a course of a disease.

Features of use:

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, arterial hypotension, nausea, vomiting, gastralgia (usually pass at a dose decline), it is rare – hypersensitivity reactions (a skin itch, an erythema, a small tortoiseshell, a Quincke's disease, a bronchospasm, an acute anaphylaxis).

Interaction with other medicines:

Tolperisonum has effect on the central nervous system, but does not cause sedation therefore it can be applied in a combination with sedative, hypnagogues, tranquilizers.

Does not strengthen effect of alcohol on the central nervous system. Increases expressiveness of effect of niflumovy acid therefore at their simultaneous use it is possible to lower a dose of the last.

Medicines for the general anesthesia, peripheral muscle relaxants, psychoactive medicines, a clonidine strengthen effect.

Contraindications:

Myasthenia, age up to 18 years, hypersensitivity to drug components, pregnancy, the lactation period. Due to the existence in composition of lactose, patients with a lactose intolerance, deficit of lactase or glyukozo-galaktozny malabsorption should not accept drug.

Overdose:

Symptoms: respiratory depression and cordial activity, lowering of arterial pressure.

Treatment: symptomatic.

Storage conditions:

In the dry, protected from light place, at a temperature not above 25 °C. To store in the place, unavailable to children! A period of validity - 2 years. Not to use after the period of validity specified on packaging.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated 50 mg and 150 mg. On 5, 7, 10, 14, 15, 20, 30 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3 or 4 blister strip packagings together with the application instruction place in a pack from a cardboard.