Tolperil solution for injections 1ml. №5


Symptomatic treatment of muscle spasm in adults after a stroke.



Composition and form of release
The main active ingredients: lidocaine hydrochloride, tolperisone hydrochloride.
Auxiliary components: ethylene glycol monoethyl ether, methylparaben, hydrochloric acid solution, water for injections.
It is issued in the form of an injection solution packed up in ampoules on 1 ml.
1 ml of the drug contains 100 mg of tolperisone hydrochloride and 2.5 mg of lidocaine hydrochloride.
Pharmacological properties
This drug belongs to the group of muscle relaxants with central action.
The effect of application is due to the properties of the main active substances – lidocaine, tolperisone hydrochloride.
The drug produces a membrane-stabilizing and local anesthetic effect, some spinal reflexes.
It also has a secondary mechanism of action due to its ability to block the release of the transmitter by blocking the entry of calcium ions into the synapses.
It is able to strengthen peripheral blood circulation, reduce the increase in muscle tone, as well as muscle rigidity, acting as an antispasmodic.
Lidocaine has such a mechanism of action, due to which it has the ability to block sodium channels. Such properties allow to stabilize a neuronal membrane, promoting decrease in its permeability, and stopping ability to conduct impulses. As a consequence, it has a rapid analgesic effect.
Due to the fact that the drug contains several active ingredients, they complement each other, produce an increased effect from its use.
This drug is used if necessary to relieve muscle cramps (spasticity). Including for relief of post-stroke spasticity in cases where the injectable form is the method of choice.
Do not use if the patient has a hypersensitivity (allergy) to one of the components that are part of the drug.
Not used for myasthenia gravis.
Contraindicated in pediatrics.
Use during pregnancy and breastfeeding
Treatment of pregnant women with this drug is contraindicated only in the first trimester. In the future, the need for the appointment is determined by the attending physician, based on the benefit / harm ratio.
Lactation should be discontinued during treatment.
Method of application and dose
For parenteral administration only.
It is intended for use only in patients over 18 years of age.
The drug is administered:

  • intramuscularly, 100 mg twice a day.
  • intravenously, once a day at 100 mg as a slow injection.

The duration of treatment is determined by the attending physician, depending on the nature of the disease and the effectiveness of treatment, the individual patient’s response to the drug.
Symptoms of overdose were observed in cases where the daily dose of the drug (in children) exceeded 300-600 mg per day.
Studies have shown that acute intoxication with high doses caused symptoms such as:

  • ataxia;
  • tonic-clonic seizures;
  • difficulty breathing until it stops.

There is no specific antidote for tolperisone.
In case of overdose, it is recommended to cancel the drug, symptomatic and supportive treatment is prescribed.
Side effects
The following side effects are possible, such as:

  • anemia, lymphadenopathy;
  • anaphylactic shock, convulsions, tremor;
  • anorexia, polydipsia;
  • insomnia, depression, headache;
  • tremor, convulsions, hyperesthesia, paresthesia;
  • tinnitus, vertigo;
  • angina, tachycardia, low blood pressure, bradycardia;
  • hypotension, redness of the skin;
  • difficulty breathing, nosebleeds, shortness of breath;
  • diarrhea, dryness of the oral mucosa, dyspepsia, nausea, epigastric pain, constipation, flatulence, vomiting.

If you experience any unusual side effects as a result of taking this drug, you should consult your doctor about possible changes in the treatment regimen.
Conditions and terms of storage
The shelf life of the drug is not more than 3 years.
This medicine should be stored in a dry place, out of reach of children, at a temperature not lower than 2 and not higher than 8 ° C.