Metadoxine

Metadoxine, also known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol intoxication. Metadoxine improves the clinical signs of acute alcohol intoxication and accelerates alcohol clearance from the blood. Metadoxine extended release is being evaluated in clinical trials as a treatment for attention deficit hyperactivity disorder (ADHD) and fragile X syndrome.
Metadoxine is an ion pair salt of pyridoxine and L-pyroglutamate (L-PGA). Pyridoxine (vitamin B6) is a precursor of coenzymes including pyridoxal 5’-phosphate (PLP), which accelerates the metabolic degradation of ethanol and prevents adenosine triphosphate (ATP) inactivation by acetaldehyde. Pyridoxal phosphate dependent enzymes also play a role in the biosynthesis of four important neurotransmitters: serotonin (5-HT), epinephrine, norepinephrine and GABA: see vitamin B6 functions. L-PGA is present in the diet and is produced endogenously by enzymatic conversion of gamma-glutamyl amino acids to L-PGA and free amino acids. In the central nervous system (CNS), L-PGA was found to have a role in composition of neuro-active molecules. Its production has been linked to hepatic gamma-glutamyl transferase activity and levels of reduced glutathione (GSH). Lastly, it was shown that L-PGA facilitates ATP synthesis by stimulating de novo synthesis of purines.