What Is Metadoxine ? – Dosage, Pregnancy Category

What Is Metadoxine ?/Metadoxine also is known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol intoxication. Metadoxine accelerates alcohol clearance from the blood. Metadoxine is an ion pair salt of pyridoxine and pyrrolidone carboxylate (PCA). 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.

The use of metadoxine in the treatment of hepatic fibrosis is described. Metadoxine can be orally and/or parenterally administered at a dosage comprised between 50 and 1000 mg per dose, preferably between 300 and 600 mg per dose. In the in vitro study, metadoxine results effectively at lower concentrations with respect to those that are obtained in the plasma after oral administration at the doses recommended for conventional pathology.

Mechanism of Action of Metadoxine

Metadoxine is a selective antagonist of the serotonin receptor subtype 5-HT_2B and displays a high affinity to the gamma-aminobutyric acid (GABA) transporter. In vitro, enzymatic assay revealed that metadoxine reduced the activity of the GABA transaminase enzyme, responsible for the degradation of GABA. Electrophysiological studies also showed that metadoxine increased inhibitory GABAergic synaptic transmission via a presynaptic effect. As it does not affect dopamine, norepinephrine or serotonin levels, metadoxine displays a novel mechanism of action as a monoamine-independent GABA modulator.^[rx]

In animal studies, metadoxine increased the activity of acetaldehyde dehydrogenase enzyme, prevented the decrease in alcohol dehydrogenase activity in chronic ethanol-fed rats, accelerated plasma and urinary clearance of ethanol, inhibited the increase of fatty acid esters in the liver of ethanol-treated rats, prevented the formation of fatty liver in rats exposed to a dose of ethanol sufficient to induce fatty liver, increased glutathione levels in the hepatocytes of acutely and chronically alcohol-intoxicated rats, prevented glutathione depletion, lipid peroxidation damage, collagen deposition, and TNF-α secretions induced by alcohol and acetaldehyde in hepatocytes and hepatic stellate cells.

Indications of Metadoxine

• Alcohol Intoxication – This medicine is used to treat alcohol intoxication (alcohol poisoning), a condition associated with drinking an excessive amount of alcohol within a short period of time. The symptoms of alcohol intoxication may include slurred speech, incoordination, mood and behavior changes, coma (in rare cases), confusion, memory loss, etc.
• Fatty liver – This medicine is used to treat alcoholic fatty liver, a condition characterized by increased deposits of fat in the liver. The symptoms of a fatty liver may include weight loss, abdominal pain, a feeling of tiredness, etc.
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