Tolperisone

Benjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.

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The active ingredient tolperisone belongs to the group of centrally acting muscle relaxants, i.e. substances that work in the brain or spinal cord to relax the muscles. In contrast to the other representatives of this group of active ingredients, tolperisone has no dampening or drowsiness-inducing effect. Here you can read everything interesting about the effects and use of tolperisone, side effects and other important facts.

This is how tolperisone works

The active ingredient tolperisone works in different places in the body, although the mechanism of action is not known down to the last detail.

Tolperisone has a similar chemical structure to lidocaine and other local anesthetics (local anesthetics). It is therefore assumed that it has a direct effect on the transmission of stimuli in the nervous system: Tolperisone is preferentially deposited in the brain, spinal cord and in the nerve tracts. Nerve cells (neurons) have long, cable-like extensions through which they are in contact with the next neuron and transmit signals. On the one hand, these signals can be sensory and can be passed from the body to the brain, such as temperature, pressure or pain stimuli. Other signals are of a motor nature: They are sent in the opposite direction from the brain to other parts of the body and trigger muscle movement, for example. The transmission of the signals along the long “cable” occurs because positively charged sodium particles enter the “cable” from outside through sodium channels, whereby a positive charge builds up inside and is transported further. Like local anesthetics, tolperisone can inhibit the entry of sodium by blocking the sodium channels. It is therefore also said that the muscle relaxant has a lidocaine-like activity.

In the case of cramp symptoms (spasticity / spasticity), the central nervous system causes an abnormally increased internal tension in the skeletal muscles. As a result, even the slightest irritation can trigger reflexes, and the muscle contracts, depending on the severity of the spasticity, sometimes very strongly, which can be associated with movement restrictions and pain. This "overdrive" by the nervous system is attempted by dampening the transmission of stimuli by tolperisone.

Tolperisone uptake, breakdown and excretion

After ingestion by mouth, the active ingredient is absorbed through the intestinal wall into the blood, where it reaches the highest level after an hour and a half. However, shortly after ingestion, four fifths of the active ingredient is broken down by the liver. If a meal is consumed before the ingestion of the active ingredient, the intake increases to about double. About two and a half hours after ingestion, half of the tolperisone and its breakdown products are excreted through the kidneys with the urine.

When is tolperisone used?

In Germany, tolperisone is only approved for the treatment of spastic symptoms after a stroke in adults.

Outside of the approved areas of application ("off-label" use) and in other countries, tolperisone is also used for other diseases such as osteoarthritis (joint wear), spondylosis (joint disease of the spine) and circulatory disorders (because it improves blood circulation).

The active ingredient is generally suitable for long-term use.

This is how tolperisone is used

The muscle relaxant tolperisone is taken in the form of tablets. The usual dosage is 50 to 150 milligrams three times a day after meals for a total dose of 150 to 450 milligrams per day.

What are the side effects of tolperisone?

Preparations with the active ingredient tolperisone are usually very well tolerated.

In clinical studies with the active ingredient, one in 100 to a thousand people treated experienced side effects such as dizziness, sleepiness, tiredness, fatigue, weakness, abdominal pain, nausea and vomiting.

Even more rarely (in one in a thousand to ten thousand patients), tolperisone caused side effects such as headache, insomnia, constipation, diarrhea, gastrointestinal complaints, reddening of the skin, rashes, itching, increased sweating and low blood pressure.

The symptoms are usually temporary or disappear when the dose is reduced. In the event of hypersensitivity reactions, the doctor should be informed and the active substance should be discontinued.

What should be considered when taking tolperisone?

The active ingredient tolperisone does not interact directly with other active ingredients. However, it is broken down in the liver by enzymes (cytochrome P450 2D6 and 2C19) that also break down other active substances. If taken at the same time, the breakdown of tolperisone or that of the other active ingredient can either be slowed or accelerated. For example, the breakdown of cardiovascular drugs from the group of beta blockers (metoprolol, nebivolol), psychotropic drugs (thioridazine, perphenazine, venlafaxine, desipramine, atomoxetine) or the cough suppressant dextromethorphan when used in combination with tolperisone slows down so that their blood levels rise sharply and Symptoms of overdose occur.

Tolperisone may also increase the effects of non-steroidal anti-inflammatory drugs, including the common over-the-counter pain relievers acetylsalicylic acid (ASA), ibuprofen, naproxen and diclofenac.

Tolperisone has caused harm to unborn babies in animal experiments, which is why it should not be taken during pregnancy. In addition, it can be assumed that the active ingredient is excreted in breast milk - breastfeeding women who absolutely must be treated with tolperisone should stop breastfeeding beforehand.

Due to the lack of experience on safety and effectiveness in children and adolescents under 18 years of age, other active ingredients should be used instead of tolperisone in minors.

In elderly patients and people with liver or kidney dysfunction, the appropriate dosage must first be carefully determined by the doctor. The active ingredient must not be used in severe liver or kidney dysfunction.

How to get drugs with tolperisone

The muscle relaxant tolperisone requires a prescription in every dosage and can be obtained from the pharmacy according to a doctor's prescription.

Since when is tolperisone known?

Tolperisone has been approved for numerous complaints in Europe since the 1960s. In 2013, the approved application areas were reduced to a single one, as severe hypersensitivity reactions rarely occurred despite the low rate of side effects. Since the expiry of patent protection, several generics with the active ingredient tolperisone have come onto the German market.

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