Midokalm (Tolperison)

Active substance:

tolperisone hydrochloride;

Excipients:

citric acid monohydrate;

silicon dioxide colloidal;

stearic acid;

talc;

MCC;

corn starch;

lactose monohydrate; 

Film sheath:

silicon dioxide colloidal;

titanium dioxide (E171-77891);

lactose monohydrate;

macrogol 6000;

hypromellose

Midokalm - muscle relaxant.

Pharmacodynamics

Muscle relaxant central action. The mechanism of action is not fully understood. It has a membrane-stabilizing, local anesthetic effect, inhibits the conduction of impulses in primary afferent fibers and motor neurons, which leads to blocking of spinal mono- and polysynaptic reflexes.

It is also likely that it slows down the release of mediators by inhibiting the entry of Ca2 + into synapses. In the brain stem eliminates the facilitation of the excitation along the reticulospinal path. Enhances peripheral blood flow regardless of the effect of the central nervous system. In the development of this effect, the weak antispasmodic and adrenoblocking effect of tolperisone plays a role.

Pharmacokinetics

After oral administration, tolperisone is well absorbed from the digestive tract. Cmax is reached after 0.5–1 h, bioavailability is about 20%.

Tolperisone is metabolized in the liver and kidneys. It is excreted in the urine in the form of metabolites (more than 99%). The pharmacological activity of metabolites is unknown.

• treatment of pathologically increased muscle tone and spasms of striated muscles resulting from organic diseases of the central nervous system (pyramidal lesions, multiple sclerosis, cerebral stroke, myelopathy, encephalomyelitis);
• treatment of increased tone and muscle spasms, muscle contractures accompanying diseases of the organs of motion (including spondylosis, spondylitis, cervical and lumbar syndromes, arthrosis of large joints);
• rehabilitation treatment after orthopedic and traumatological operations;
• in the combination therapy of obliterating vascular diseases (atherosclerosis obliterans, diabetic angiopathy, thromboangiitis obliterans, Raynaud's disease, diffuse scleroderma), diseases arising from vascular innervation disorders (acrocyanosis, intermittent angioneurotic dysbasia);
• Little's disease (cerebral palsy) and other encephalopathies accompanied by muscular dystonia.

The drug Midokalm is contraindicated in pregnancy, breast-feeding and children under 3 years of age.

• hypersensitivity to any of the components of the drug;
• myasthenia gravis.

• drowsiness, 
• nausea, 
• dizziness
• dry mouth
• constipation, 
• diarrhea, 
• pressure reduction
• feeling tired 
• sleep disorders 
• confusion.

There are no data on interactions that limit the use of the drug Midocalm.

Although tolperisone has an effect on the central nervous system, it does not cause a sedative effect, so it can be used in combination with sedatives, hypnotics and drugs containing alcohol.

Does not affect the effect of alcohol on the central nervous system.

Tolperisone enhances the effect of niflumic acid, while the use of these drugs may require a reduction in the dose of niflumic acid.

Means for general anesthesia, peripheral muscle relaxants, psychotropic drugs, clonidine - enhance the effect of tolperisone.

In most cases, adults are prescribed 150 mg 3 times a day.

For children aged 1 year to 6 years, Midokalm is prescribed orally in a daily dose at the rate of 5-10 mg / kg (in 3 doses during the day); at the age of 7-14 years - in a daily dose of 2-4 mg / kg in 3 divided doses.

There have been no reports of an overdose of Midokalm.

Apply strictly as directed by your doctor to avoid complications.

Influence on the ability to drive vehicles and mechanisms. 

No studies have been conducted, but such information has not been reported over many years of use of the drug.

Tablets.