Mexiletine hydrochloride
The clinical term myotonia is used to identify a series of dominant and recessive forms of genetic skeletal muscle diseases characterized by abnormal membrane excitability and delayed muscle relaxation after voluntary contraction. Sodium channel myotonias, paramyotonia congenita, and hyperkaliemic periodic paralysis are due to mutations of the gene coding for the skeletal muscle type of voltage-gated sodium channels.
Mexiletine, an orally effective antiarrhythmic drug of the IB class with use-dependent sodium channel-blocking properties, is used for the treatment of ventricular arrhythmia. Also, it is among the few drugs used to reduce or prevent myotonia, to treat long QT-3 syndrome and to alleviate neuropathic pain.
Mexiletine presents IC50 values ranging from ~50 uM to ~100 uM and from ~20 uM to ~30 uM for tonic and phasic block, respectively, on single muscle fibers and a value of 253 uM in HEK293 cells.
Mexiletine has a neuroprotective feature against cerebral ischemia, spinal trauma and head trauma. In addition, it protects the neuronal tissue against diabetic oxidative damage.
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