Products
Flupirtine is not approved as a drug in many countries. In some European countries, it was commercially available in the form of capsules and suppositories (e.g., Katadolon, Trancopal Dolo), among others. In Germany, flupirtine had been registered since 1989. In 2018, it was withdrawn from the market due to liver toxicity.
Structure and properties
Flupirtine (C15H17FN4O2, Mr = 304.3 g/mol) is present in the drug as flupirtine maleate. It is a carbamate and pyridine derivative.
Effects
Flupirtine (ATC N02BG07) has central analgesic and muscle relaxant properties and has an effect on “pain memory.” The effects are due to the opening of potassium channels and inhibition of activation of nerve cells. Flupirtine belongs to the so-called SNEPCO (Selective NEuronal Potassium Channel Openers).
Indications
For the treatment of acute and chronic pain.
Dosage
According to the professional information. Capsules are usually taken three to four times daily. Flupirtine has a medium-long half-life of 7 to 10 hours.
Contraindications
For complete information on precautions and drug interactions, see the Drug Information Leaflet.
Adverse effects
The most common possible adverse effects include fatigue, loss of appetite, dizziness, tremor, headache, indigestion, and sweating. Liver disorders such as transaminase elevations, hepatitis, and liver failure (isolated cases) have been reported rarely. The European Medicines Agency had announced a review in March 2013 due to the hepatic side effects, as increased cases were reported in Germany. Market withdrawal followed in 2018.