Tolperizone-OBL, 150 mg 30 pcs

Pharmacodynamics

Tolperizone-OBL is a myorelaxant of the central mechanism of action. It has membrane stabilizing effect, inhibits conduction of nerve impulses in primary afferent fibers and motor neurons, which leads to blocking of spinal mono- and polysynaptic reflexes. Probably mediates the blocking of mediator release by inhibition of Ca⁺² entry into synapses. Inhibits the conduction of excitation along the reticulospinal pathway in the brainstem.

Independent of central nervous system effects, it enhances peripheral blood flow. The weak antispasmodic and antiadrenergic effect of tolperizone may play a role in the development of this effect.

Pharmacokinetics

After oral administration tolperizone is well absorbed from the small intestine. Maximal concentration in blood plasma is reached 30 minutes to 1 hour after intake, bioavailability due to marked presystemic metabolism is about 20%. Tolperisone is extensively metabolized in the liver and kidneys. It is excreted with urine almost exclusively (more than 99%) as metabolites. 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 tracts, multiple sclerosis, stroke, myelopathy, encephalomyelitis).

Treatment of increased tone and muscle spasms, muscle contractures accompanying diseases of the musculoskeletal system (spondylosis, spondyloarthrosis, arthrosis of large joints, cervical and lumbar pain syndromes).

Rehabilitation treatment after surgical interventions in orthopedics and traumatology.

As part of combination therapy for obliterating vascular diseases (obliterating atherosclerosis, diabetic angiopathy, thromboangiitis obliterans, Raynaud’s disease), as well as diseases resulting from impaired vascular innervation (acrocyanosis, intermittent angioedema).

Pharmacological effect

Pharmacodynamics

Tolperisone-OBL is a muscle relaxant with a 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. Inhibits the conduction of excitation along the reticulospinal tract in the brain stem.

Regardless of the influence of the central nervous system, it increases peripheral blood flow. The weak antispasmodic and antiadrenergic effect of tolperisone may play a role in the development of this effect.

Pharmacokinetics

After oral administration, tolperisone is well absorbed from the small intestine. The maximum concentration in the blood plasma is reached 30 minutes – 1 hour after administration; bioavailability due to pronounced first-pass metabolism is about 20%. Tolperisone is extensively metabolized in the liver and kidneys. Excreted in urine almost exclusively (more than 99%) in the form of metabolites. The pharmacological activity of the metabolites is unknown.

Special instructions

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Active ingredient

Tolperisone

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 (hydroxypropylcellulose), crospovidone, stearic acid

Excipients for coating: Opadry II (Series 85) [polyvinyl alcohol, macrogol (polyethylene glycol), talc, titanium dioxide]

Pregnancy

The drug Tolperisone-OBL is contraindicated during pregnancy, breastfeeding and children under 3 years of age.

Contraindications

myasthenia gravis,
hypersensitivity to the components of the drug.

Due to the presence of lactose, patients with lactose intolerance, lactase deficiency or glucose-galactose malabsorption should not take the drug.

Side Effects

muscle weakness,
headache,
arterial hypotension,
nausea,
vomit,
gastralgia (usually disappears with dose reduction),
rarely – hypersensitivity reactions (itching, erythema, urticaria, angioedema, bronchospasm, anaphylactic shock).

Interaction

Tolperisone has an effect on the central nervous system, but does not cause a sedative effect, therefore it can be used in combination with sedatives, hypnotics, and tranquilizers. Does not enhance the effect of alcohol on the central nervous system.

Increases the severity of the action of niflumic acid, so when used simultaneously, the dose of the latter can be reduced.

medications for general anesthesia, peripheral muscle relaxants, psychoactive drugs, clonidine enhance the effect.

Overdose

Symptoms: respiratory and cardiac depression, decreased blood pressure.

Treatment: symptomatic.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 °C

Shelf life

2 years.

Manufacturer

Alium JSC, Russia