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Mephenesin is a centrally acting muscle relaxant that primarily depresses the central nervous system, particularly the spinal cord and brainstem. It functions by inhibiting polysynaptic reflex arcs, which are responsible for muscle spasms, thereby reducing muscle tension and spasticity without directly interfering with neuromuscular transmission or muscle function. Its mechanism also involves enhancing GABAergic transmission, reducing the release of excitatory neurotransmitters like glutamate, and blocking inward sodium and calcium currents in central neurons. Mephenesin may also act as an NMDA receptor antagonist. Historically, it was used for muscle relaxation during surgical anesthesia, tetanus, strychnine poisoning, and to alleviate muscle spasms in neurological disorders such as Parkinson's disease and multiple sclerosis. While it has a short duration of action and has been largely replaced by more effective alternatives like methocarbamol in many regions, it remains available in some countries, including Italy and the Philippines. It is no longer available in North America, and Sanofi Aventis ceased its production in France in July 2019.
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