Tolperisone

Products

Tolperisone is commercially available in the form of film-coated tablets (Mydocalm, generic). It has been approved in many countries since 1966.

Structure and properties

Tolperisone (C16H23NO, Mr = 245.36 g/mol) is chiral and is present in drugs as racemate and tolperisone hydrochloride. It is a piperidine derivative and a propiophenone. Tolperisone has structural similarities to lidocaine and a similar mechanism of action to the local anesthetic.

Effects

Tolperisone (ATC M03BX04) has central muscle relaxant properties on striated skeletal muscle. It decreases peripheral muscle tone in the brainstem. the molecular drug targets are likely sodium and calcium channels. Unlike other muscle relaxants such as tizanidine (Sirdalud, generics), tolperisone is not depressant, so it does not elicit fatigue as an adverse effect. Tolperisone has a short half-life of 1.5 to 2.5 hours. In many countries and some European countries, the drug is used comparatively frequently and widely. However, the European Medicines Agency (EMA) concluded in 2012 that while the benefits outweigh the risks, tolperisone should be used solely for post-stroke spasticity. Studies conducted in the 1960s and 1970s do not fully meet today’s requirements.

Indications

European Medicines Agency recommendation:

In many countries, the following indications are still currently valid:

  • Muscle spasms in painful diseases of the skeletal muscles, especially the spine and joints near the trunk.
  • May be used for increased skeletal muscle tone in neurological disorders such as pyramidal tract lesions.

Dosage

According to the professional information. Adults usually take 150 mg three times daily. The maximum daily dose is 600 mg. Dose adjustments are needed in some patient groups.

Contraindications

  • Hypersensitivity
  • Myasthenia gravis
  • Lactation

Patients must be informed that during treatment, hypersensitivity reactions can occur with a severe course. When they occur, therapy should be interrupted. Full precautions can be found in the drug information leaflet.

Interactions

Tolperisone is metabolized primarily by CYP2D6, and to a lesser extent by other CYP isozymes. Corresponding drug-drug interactions are possible.

Adverse effects

Occasional possible adverse effects include dizziness, loss of balance, tremor, paresthesias, palpitations, hypotension, dry mouth, nausea, diarrhea, vomiting, abdominal pain, flatulence, sweating, hives, and skin flushing. In rare cases, severe hypersensitivity reactions are possible. These reactions may occur suddenly even after years of taking the drug.