How tolperisone works
Tolperisone acts at different sites in the body, although its mechanism of action is not yet known in detail.
The active ingredient has a similar chemical structure to lidocaine and other local anesthetics. Therefore, it is thought to have a direct effect on the conduction of stimuli in the nervous system, most likely through sodium and calcium channels (tolperisone accumulates preferentially in the brain, spinal cord, and nerve tracts).
Nerve cells (neurons) have long cable-like extensions by which they contact the next neuron and transmit signals. On the one hand, these signals can be sensory and carried from the body to the brain such as temperature, pressure or pain stimuli. Other signals are motor in nature. They are sent in the opposite direction from the brain to other parts of the body and trigger a muscle movement, for example.
In the case of spasm symptoms (spasticity/spasticity), the central nervous system causes an abnormally increased inherent tension of the skeletal muscles. As a result, even reflexes can be triggered by the slightest irritation, and the muscle contracts, sometimes very severely, depending on the severity of the spasticity. This is usually associated with movement restrictions and pain.
Attempts are made to counteract this “overdrive” by the nervous system by dampening the transmission of stimuli with tolperisone.
Absorption, degradation and excretion
After ingestion by mouth, the drug is absorbed through the intestinal wall into the blood, where it reaches its highest levels after one and a half hours. However, four-fifths of the active ingredient is broken down by the liver shortly after absorption.
When is tolperisone used?
In Germany, tolperisone is approved only for the treatment of spastic symptoms following stroke in adults.
In Switzerland, there are additional indications for this active ingredient: muscle spasms in painful diseases of the skeletal musculature, especially of the spine and the joints close to the trunk, and increased tension (tone) of the skeletal musculature in neurological diseases.
Outside of approved indications (“off-label”) and in other countries, tolperisone is also used for other conditions such as osteoarthritis (joint wear), spondylosis (joint disease of the spine), and circulatory disorders (tolperisone improves blood flow).
The active ingredient is generally suitable for long-term use.
How tolperisone is used
What are the side effects of tolperisone?
Preparations containing tolperisone are usually very well tolerated.
In clinical trials with the drug, one in one hundred to one thousand people treated experienced side effects in the form of dizziness, drowsiness, fatigue, faintness, weakness, abdominal pain, nausea, and vomiting.
Even more rarely (in one in a thousand to ten thousand patients), tolperisone caused headache, insomnia, constipation, diarrhea, gastrointestinal discomfort, skin redness, rash, itching, increased sweating, and low blood pressure as side effects.
The symptoms are usually temporary or disappear when the dose is reduced.
Very rarely, severe hypersensitivity reactions have been reported. These can occur suddenly even after years of regular use and are the reason why the European Medicines Agency has restricted the indications for tolperisone (for the EU area).
What should be considered when taking tolperisone?
Contraindications
Tolperisone must not be used in the following cases:
- hypersensitivity to the active substance or to any of the other components of the drug
- myasthenia gravis (abnormal muscle weakness)
- Lactation
Drug interactions
The active substance tolperisone does not interact directly with other active substances. However, it is broken down in the liver by certain enzymes (cytochrome P450 2D6 and 2C19) that also break down other active ingredients. When taken at the same time, the breakdown of tolperisone or that of the other active ingredient may therefore either be slowed down or accelerated.
Conversely, tolperisone may increase the effects of nonsteroidal anti-inflammatory drugs (NSAIDs), which include the common pain relievers acetylsalicylic acid (ASA), ibuprofen, naproxen, and diclofenac.
Age restriction
Because of the lack of experience on safety and efficacy in minors, children and adolescents should preferably receive other agents instead of tolperisone.
In elderly patients and those with liver or kidney dysfunction, the appropriate dosage must first be carefully determined by the physician.
Pregnancy and lactation
No data are available on the use of tolperisone in pregnancy. Animal studies have shown no evidence of an increased risk of malformation (teratogenic risk) in the unborn child. However, to be on the safe side, the drug should not be used during pregnancy – unless the physician considers the expected benefits to be greater than the potential risks.
How to obtain medication with tolperisone
Tolperisone is available by prescription in Germany and Switzerland in any dosage and can be obtained from pharmacies after a doctor’s prescription. There are currently no medicines with the active ingredient tolperisone registered in Austria.
Since when is tolperisone known?
Tolperisone has been approved in Europe for numerous complaints since the 1960s. In 2012, the approved indications in the EU were reduced to one, as severe hypersensitivity reactions rarely occurred despite the low side effect rate.
Since patent protection expired, several generics with the active ingredient tolperisone have entered the German market.
