Tolperisone - instructions for use, doses, side effects, contraindications

Selective oppression of the caudal part of the reticular formation of the brain. Reduces the pathologically increased tone of skeletal muscles. Has central n-anticholinergic properties.

Pharmacokinetics:

Absorbed in the small intestine. F - 17%. Biotransformation in the liver, the effect of the first passage through the liver. Half-life with intravenous administration is 1.5 hours, with oral administration - 2.5 hours. TCmax 0.5-1 hour. Elimination by the kidneys for 24 hours (less than 0.1% unchanged).

Indications:

Spinal and cerebral palsy (hypertonus, muscle spasm, spinal automatism, limb contracture).

Diseases accompanied by dystonia, stiffness, muscle spasm; obliterating arterial diseases: obliterating atherosclerosis of the vessels of the extremities, diabetic angiopathy, obliterating thromboangiitis (Buerger's disease),Raynaud's syndrome.

Consequences of disorders of vascular innervation (acrocyanosis, intermittent angioedema dysbasia).

Extrapyramidal disorders (postencephalitic and atherosclerotic parkinsonism).

Post-thrombotic disorders of lymph circulation and venous circulation, trophic ulceration of the lower leg, children's spastic paralysis (Little's disease), epilepsy, encephalopathy of vascular genesis; Hypertension in combination with a violation of muscle tone of another type.

ICD-10

VI.G20-G26.G21 Secondary Parkinsonism

VI.G40-G47.G40 Epilepsy

VI.G80-G83.G80 Cerebral palsy

VI.G80-G83.G81 Hemiplegia

VI.G80-G83.G82.1 Spastic paraplegia

VI.G80-G83.G82.4 Spasmodic tetraplegia

IX.I70-I79.I73.0 Raynaud's syndrome

IX.I70-I79.I73.1 Obliterating thromboangitis [Berger's disease]

IX.I70-I79.I73.9 Peripheral vascular disease, unspecified

IX.I70-I79.I79.2 * Peripheral angiopathy in diseases classified elsewhere

XVIII.R25-R29.R25.2 Cramp and spasm

Contraindications:

Hypersensitivity, myasthenia gravis, pregnancy, breast-feeding; children under 1 year.

Carefully:Patients with renal and hepatic insufficiency. Correction of the dose is not required.

Pregnancy and lactation:

Adequate and well-controlled studies in humans and animals have not been conducted. Do not apply! There is no information on the penetration into breast milk. Do not apply!

Category of recommendations FDA is not defined.

Dosing and Administration:

When administered orally, the initial dose is 50 mg 2-3 times / day; The dose is gradually increased to 150 mg 2-3 times / day. In / m - on 100 mg 2 times / sut; in / in - 100 mg / day once.

Children aged 1 to 6 years - inside at a dose of 5 mg / kg / day in 3 divided doses; at the age of 7-14 years - inside in a dose of 2-4 mg / kg 3 times / day.

Side effects:

Possible: headache, myasthenia gravis, arterial hypotension, nausea, vomiting, gastralgia, allergic reactions (anaphylactic shock, bronchospasm, urticaria, erythematous rashes, itchy skin).

Overdose:

Symtomas: depression of respiration and cardiac activity, reduction of blood pressure.

Treatment: symptomatic.

Interaction:

Medicines for general anesthesia, peripheral muscle relaxants, psychoactive drugs, clonidine - Increased myorelaxing effect.

Special instructions:

With nonspecific pain in the lumbar region, central muscle relaxants can be effective, but studies are needed,To assess the adverse effects of their action and compare them with anesthetics and NSAIDs.

Not listed in the US Pharmacopeia

Instructions

Tolmoreyson (Tolperisonum)