Description
Latin name
Tolperizon-OBL
Release form
Film-coated tablets.
Packing
30 pcs
Pharmacological action
Pharmacodynamics
Tolperisone-OBL – muscle relaxant of the central mechanism of action. It has a membrane stabilizing effect, inhibits the conduction of nerve impulses in primary afferent fibers and motor neurons, which leads to blocking of spinal mono- and polysynaptic reflexes. Probably, mediates blocking the release of mediators by inhibiting the entry of Ca + 2 into synapses. It inhibits the conduction of excitation along the reticulospinal path in the brain stem.
Regardless of the influence of the central nervous system, it enhances peripheral blood flow. In the development of this effect, the weak antispasmodic and antiadrenergic effect of tolperisone may play a role.
Pharmacokinetics
After oral administration, tolperisone is well absorbed from the small intestine. The maximum concentration in blood plasma is reached after 30 minutes – 1 hour after administration, bioavailability due to pronounced presystemic metabolism is about 20%. Tolperisone is extensively metabolized in the liver and kidneys.
Excreted in the urine almost exclusively (over 99%) as metabolites. The pharmacological activity of metabolites is unknown.
Indications
Treatment of pathologically increased tone and spasms of striated muscles caused by organic neurological pathology (including damage to the pyramidal pathways, multiple sclerosis, stroke, myelopathy, encephalomyelitis).
Treatment of increased tone and muscle spasms, muscle contractures accompanying diseases of the musculoskeletal system (spondylosis, spondylitis, arthrosis of large joints, cervical and lumbar pain syndromes).
Reconstructive treatment after surgical interventions in orthopedics and traumatology.
As part of the combination therapy of obliterating vascular diseases (atherosclerosis obliterans, diabetic angiopathy, thromboangiitis obliterans, Raynaud’s disease), as well as diseases arising from impaired vascular innervation (acrocyanosis, intermittent angioneurotic dysbasia).
Contraindications
hypersensitivity (including to lidocaine),
myasthenia gravis,
childhood (up to 1 year).
Use during pregnancy and lactation
Contraindicated during pregnancy and lactation.
Composition
1 tablet contains:
active substance:
tolperisone hydrochloride – 50 mg (for dosage 50 mg) or 150 mg (for dosage 150 mg)
excipients:
citric acid,
lactose monohydrate (milk) hyprolose (hydroxypropyl cellulose),
crospovidone,
stearic acid
coating aids:
Opadry II (Series 85) [polyvinyl alcohol, macrogol (polyethylene glycol), talc, titanium dioxide]
Dosage and Administration
Inside.
For adults, the initial dose is 50 mg 2-3 times a day, with a gradual increase to 150 mg 2-3 times a day.
The duration of treatment depends on the severity and nature of the course of the disease.
Side effects
headache,
myasthenia gravis,
decreased blood pressure,
nausea,
vomiting,
gastralgia,
allergic reactions (anaphylactic shock, bronchospasm, urticaria, erythematous rashes, skin itching).
Drug interaction
drugs for general anesthesia, peripheral muscle relaxants, psychoactive drugs, clonidine enhance the effect.
Overdose
Symptoms: respiratory depression and cardiac activity, decreased blood pressure.
Treatment: symptomatic.
Storage conditions
Store at room temperature.
Expiration
2 years.
pharmacy terms with prescription
Dosage
form Dosage form
tablets
Obolenskoye FPP, Russia
