Product Overview
Composition
1 tablet contains:
active substance: tolperisone hydrochloride - 50 mg (for a dosage of 50 mg) or 150 mg (for a dosage of 150 mg);
excipients: citric acid, lactose monohydrate (milk sugar), hyprolose (hydroxypropyl cellulose), crospovidone, stearic acid
excipients for the shell: Opadry II (Series 85) [polyvinyl alcohol, macrogol (polyethylene glycol), talc, titanium dioxide]
pharmachologic effect
Tolperisone-OBL is a 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. It is likely to mediate the blocking of 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 presystem metabolism is about 20%. Tolperisone is extensively metabolized in the liver and kidneys. Excreted in the urine almost exclusively (more than 99%) in the form of metabolites. The pharmacological activity of metabolites is unknown.
Indications
Treatment of increased tone and muscle spasms, muscle contractures accompanying diseases of the musculoskeletal system (spondylosis, spondylarthrosis, 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).
Pregnancy and lactation
The drug Tolperisone-OBL is contraindicated in pregnancy, breast-feeding and children under 3 years of age.
Contraindications
- myasthenia gravis
- hypersensitivity to the components of the drug.
Due to the presence of lactose in the composition, patients with lactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take the drug.
Side effects
- muscle weakness
- headache,
- arterial hypotension,
- nausea,
- vomiting
- gastralgia (usually go away with a lower dose)
- rarely - hypersensitivity reactions (skin itching, erythema, urticaria, angioedema, bronchospasm, anaphylactic shock).
Interaction
Tolperisone has an effect on the central nervous system, but does not cause a sedative effect, so it can be used in combination with sedatives, hypnotics, tranquilizers. Does not increase the effect of alcohol on the central nervous system.
It increases the severity of the action of niflumic acid, therefore, with their simultaneous use, the dose of the latter can be reduced.
Drugs for general anesthesia, peripheral muscle relaxants, psychoactive drugs, clonidine enhance the effect.
How to take, course of administration and dosage
Inside. For adults, the initial dose of 50 mg 2-3 times a day, with a gradual increase to 150 mg 2-3 times a day. The duration of the course of treatment depends on the severity and nature of the course of the disease.
Overdose
Symptoms: respiratory depression and cardiac activity, lowering blood pressure.
Treatment: symptomatic.
Special instructions
During the treatment period, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
Release form
Film-coated tablets
