Flupirt

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 flupirtine has an analgesic and muscle-relaxing effect. Although it works in the central nervous system (brain and spinal cord), it is not an opioid and cannot be assigned to any other class of pain relievers. Here you can read everything you need to know about the effects and use of flupirtine, side effects and interactions.

This is how flupirtine works

The active ingredient flupirtine has a threefold mechanism of action.

The analgesic effect comes about through the action at the interfaces (synapses) of nerve cells that guide the pain stimulus from the body to the brain. Electrical signals that reach the synapses and are then transferred to the next nerve cell with the help of messenger substances are transported via these interconnects. The stimulus is only passed on from a certain concentration of messenger substances (“all-or-nothing law”). Flupirtin raises the threshold even further, which means that stimuli are passed on even less and possibly no longer at all.

The muscle relaxing effect of flupirtine is based on a similar mechanism. Nerve impulses from the brain to the muscle are only passed on in a weakened manner. Because the active ingredient works primarily on heavily used muscles, muscle tension is released in a targeted manner, but there is no general muscle relaxation.

As a third effect, flupirtine also works against the chronification of pain, i.e. the permanent presence of pain. If pain lasts longer than three to six months, a so-called pain memory is formed: nerve cells become more and more sensitive as a result of persistent pain stimuli, which means that their pain threshold drops. Even a light touch can then be felt as pain. Flupirtin counteracts this mechanism by raising the threshold for stimulus transmission and thereby normalizing it again.

Uptake, breakdown and excretion of flupirtine

After ingestion, the active ingredient is absorbed from the intestine into the blood and thus reaches its place of action. About three quarters are broken down in the liver into less effective and ineffective substances, a quarter is excreted unchanged. Most of the active ingredient is excreted via the kidneys with the urine, and a smaller part is also excreted in the bile with the stool. About seven hours after ingestion, the blood level of flupirtine fell by half again.

When is flupirtine used?

The pain reliever is used to treat acute pain in adults when treatment with other pain relievers (NSAIDs such as ASA, ibuprofen, diclofenac, metamizole; weak opioids such as tramadol, tilidine) is not an option.

Because of its muscle-relaxing effect, the active ingredient is often prescribed for orthopedic ailments.

Treatment should not exceed two weeks.

This is how flupirtine is used

When taking flupirtine hard capsules, the dosage is 100 milligrams of the active ingredient three to four times a day. If the pain is severe, the single dose can be increased to 200 milligrams. However, a total daily dose of 600 milligrams must not be exceeded.

Extended-release tablets containing 400 milligrams of flupirtine, which slowly release their active ingredient throughout the day, only need to be taken once a day.

Because of the slightly lower intake of flupirtine as a suppository, the single dose of this dosage form is 150 milligrams three to four times a day. The maximum daily dose is 900 milligrams.

What are the side effects of flupirtine?

In more than ten percent of patients, flupirtine increases certain levels of enzymes in the blood (transaminases) and makes them tired, especially at the beginning of treatment.

One in ten to one hundred people treated develops dizziness, heartburn, nausea, vomiting, stomach upset, constipation, diarrhea, gas, increased sweating, sleep disorders, loss of appetite, depression, tremors, headache, stomach pain, dry mouth and nervousness.

Side effects that affect the gastrointestinal tract, fatigue, dark urine, jaundice and itching, in particular, can be signs of severe liver damage. In this case, the use of flupirtine must be stopped and a doctor should be consulted.

In individual cases a harmless green coloration of the urine is possible.

What should be considered when taking flupirtine?

Taking flupirtine at the same time as other active ingredients that have calming or muscle-relaxing properties can increase the effects of flupirtine. This applies, for example, to sedatives and sleeping pills, agents for epilepsy and convulsions, as well as alcohol.

Flupirtine is transported in the blood via transport proteins (albumin), which also transport other drugs. If taken at the same time, flupirtine may displace the other substances from the blood, making them more effective. Studies indicate that this is the case with sedatives and sleeping pills from the class of benzodiazepines (diazepam, lorazepam, lormetazepam) and anticoagulants of the coumarin type (warfarin, phenprocoumon).

The combination with other active substances that damage the liver (paracetamol, carbamazepine, alcohol) should be avoided.

Since only limited data on tolerability and safety are available for use during pregnancy and breastfeeding, flupirtine should not be taken during this time. The active ingredient is also not approved for children and adolescents under 18 years of age.

Elderly patients and patients with kidney or liver problems should only take a reduced dose of flupirtine.

How to get flupirtine medication

In Germany, flupirtine is only available on prescription in any dosage.

Since when is Flupirtin known?

The active ingredient flupirtine was developed from 1961 by the German chemist Walter von Bebenburg at the chemical company Degussa AG and marketed in Europe from 1984 by the pharmaceutical company Asta Medica AG (formerly Chemiewerk Homburg). Flupirtine was never approved in the US drug market. In the meantime, there are also some generics with the active ingredient flupirtine on the market in this country.

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