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

The 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).

Restorative treatment after surgical interventions in orthopedics and traumatology.

In the combined therapy of obliterating vascular diseases (obliterating atherosclerosis, diabetic angiopathy, obliterating thrombangiitis, Raynaud’s disease), as well as diseases due to disorders of vascular innervation (acrocyanosis, intermittent angioneurotic dysbasia).

Active ingredient

Composition

1 tablet contains:

the active ingredient: tolperizone hydrochloride – 50 mg (for dosage 50 mg) or 150 mg (for dosage 150 mg);

excipients: citric acid, lactose monohydrate (milk sugar), hyprolose (hydroxypropyl cellulose), crosspovidone, stearic acid

coating aids: Opadray II (Series 85) [polyvinyl alcohol, macrogol (polyethylene glycol), talc, titanium dioxide]

How to take, the dosage

Ingestion. In adults the initial dose is 50 mg 2-3 times a day with gradual increase to 150 mg 2-3 times a day. The duration of treatment depends on the severity and nature of the disease.

Interaction

Tolperizone has an effect on the central nervous system, but does not cause sedation, so it can be used in combination with sedatives, sleeping pills, tranquilizers. It does not increase the effect of alcohol on the central nervous system.

It increases the severity of the effects of niflumic acid, so if they are used concomitantly, the dose of the latter can be reduced.

The drugs for general anesthesia, peripheral myorelaxants, psychoactive drugs, clonidine increase the effect.

Special Instructions

During treatment, caution should be exercised when driving motor vehicles and engaging in other potentially dangerous activities that require increased concentration and quick psychomotor reactions.

Contraindications

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

Side effects

Overdose

Symptoms: respiratory and cardiac depression, decreased blood pressure.

Treatment: symptomatic.

Pregnancy use

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

Similarities