Open Access Articles- Top Results for Metadoxine


Systematic (IUPAC) name
L-Proline, 5-oxo-, compd. with 5-hydroxy-6-methylpyridine-3,4-dimethanol (1:1)
Clinical data
Oral, IV
ChemSpider 23089666
Chemical data
Formula C13H18N2O6
298 g/mol
 14pxN (what is this?)  (verify)

Metadoxine, also known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol abuse.[1] Metadoxine improved the clinical signs of acute alcohol intoxication and accelerated alcohol clearance from the blood [2]It is in human clinical trials as an attention-deficit/hyperactivity disorder predominantly inattentive treatment.[3]

Pyridoxine is an ion pair salt of a vitamin B6 form and of a precursor to the metabolically active pyridoxal phosphate. Pyridoxal phosphate is a coenzyme to many enzymes: see vitamin B6 metabolic functions.

Pyrrolidone carboxylate is involved in amino acid metabolism through the glutathione pathway.[4] Glutathione is an important antioxidant and combats redox imbalance. It also supports de novo ATP synthesis.[5]


Metadoxine is predominantly used in developing nations for acute alcohol intoxication. Alternate names include: Abrixone (Eurodrug, Mexico), Alcotel (Il Yang, South Korea), Ganxin (Qidu Pharmaceutical, China), Metadoxil (Baldacci, Georgia; Baldacci, Italy; Baldacci, Lithuania; CSC, Russian Federation; Eurodrug, Colombia; Eurodrug, Hungary; Eurodrug, Thailand; Micro (HC, India), Viboliv (Dr. Reddy's, India), Alcoliv (India) and Xin Li De (Zhenyuan Pharm, China).[6]


Treatment for acute alcohol abuse

In an animal model, metadoxine treatment increased the clearance of alcohol and acetaldehyde, reduced the damaging effect of free radicals, and enabled cells to restore cellular ATP and glutathione levels. [7][8] It increases the urinary elimination of ketones, which are formed when the oxidation rate of acetaldehyde into acetate is exceeded on massive alcohol intoxication.[8][4]

As a medical treatment, it is typically given intravenously.

Treatment for AD/HD-PI

Metadoxine is a selective antagonist to the 5-HT2B receptor, a member of the serotonin receptor family.[3] Electrophysiological studies also showed that Metadoxine caused a dose-dependent, reversible reduction in glutamatergic excitatory transmission and enhancement of GABAergic inhibitory transmission, changes that may be associated with cognitive regulation.[3] It is given orally in an extended release pill, which differs from the instant release alcohol treatment.

Treatment for liver disease

Metadoxine may block the differentiation step of preadipocytes by inhibiting CREB phosphorylation and binding to the cAMP response element, thereby repressing CCAAT/enhancer-binding protein b during hormone-induced adipogenesis.[7]

Treatment for Fragile X Syndrome

Metadoxine treatment led to significant improvement in blood and brain biological markers (AKT and ERK), which may have a role in learning and memory.[3] The study also demonstrated a reduction in the amount of immature neurons and abnormally increased protein levels.[3]


  1. ^ Addolorato, G; Ancona C; Capristo E; Gasbarrini G (2003). "Metadoxine in the treatment of acute and chronic alcoholism: a review". International Journal of Immunopathology and Pharmacology. 
  2. ^ Martinez, Diaz; Villamil Salcedo; Cruz Fuentes (2001). "Efficacy of Metadoxine in the Management of Acute Alcohol Intoxication". Journal of International Medical Research. 
  3. ^ a b c d e "Metadoxine extended release (MDX) for adult ADHD". Alcobra Ltd. 2014. Retrieved 2014-05-07. 
  4. ^ a b Shpilenya, Leonid S.; Alexander P. Muzychenko; Giovanni Gasbarrini; Giovanni Addolorato (2002). "Metadoxine in Acute Alcohol Intoxication: A Double-Blind, Randomized, Placebo-Controlled Study". Alcoholism:Clinical and Experimental Research. 
  5. ^ Shull, Kenneth H.; Robert Kisilevsky (1996). "Effects of Metadoxine on cellular status of glutathione and on enzymetric defence system following acute ethanol intoxication in rats". Drugs Exp Clin Res. 
  6. ^ "Metadoxine -". 2014. Retrieved 2014-05-08. 
  7. ^ a b Yang, YM; HE Kim; SH Ki; SG Kim (2009). "Metadoxine, an ion-pair of pyridoxine and L-2-pyrrolidone-5-carboxylate, blocks adipocyte differentiation in association with inhibition of the PKA-CREB pathway.". Archives of Biochemistry and Biophysics 488: 91–99. doi:10.1016/ 
  8. ^ a b Calabrese, V; A Calderone; N Ragusa; V Rizza (1971). "Effects of l-2-pyrrolidone-5-carboxylate on hepatic adenosine triphosphate levels in the ethionine-treated rat". Biochemical Pharmacology 20: 2781–5. PMID 5114511. doi:10.1016/0006-2952(71)90188-2.