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Metadoxine
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Metadoxine
Metadoxine, also 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.
As a treatment for alcohol intoxication and liver disease, metadoxine is typically given intravenously as immediate release formulation.[citation needed]
In clinical studies, metadoxine has been reported to reduce the half-life of ethanol in healthy volunteers and in acutely intoxicated patients; to accelerate the metabolism of alcohol and acetaldehyde into less toxic higher ketones and to improve their urinary clearance; to restore laboratory variables such as alcohol, ammonia, γ-GT, and alanine aminotransferase; and to improve clinical symptoms of alcohol intoxication, including psychomotor agitation, depression, aggressiveness, and equilibrium disorders. There is also evidence that metadoxine has an effect on reducing craving for alcohol. Data from clinical studies also support an effect of metadoxine on reducing indices of liver cell necrosis and fat accumulation in alcoholic fatty liver.
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. Metadoxine, when given in an immediate release form in doses from 300 mg twice a day to 500 mg three times a day of up to 3 months, has been shown to improve biochemical indices of liver function as well as reduce ultrasonic evidence of fatty liver disease.
Metadoxine is a selective antagonist of the serotonin receptor subtype 5-HT2B and displays 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.
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.
Metadoxine is predominantly used as metadoxine immediate release formulation in developing nations for acute alcohol intoxication and chronic alcoholic liver disease. Alternate names include:
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Metadoxine
Metadoxine, also 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.
As a treatment for alcohol intoxication and liver disease, metadoxine is typically given intravenously as immediate release formulation.[citation needed]
In clinical studies, metadoxine has been reported to reduce the half-life of ethanol in healthy volunteers and in acutely intoxicated patients; to accelerate the metabolism of alcohol and acetaldehyde into less toxic higher ketones and to improve their urinary clearance; to restore laboratory variables such as alcohol, ammonia, γ-GT, and alanine aminotransferase; and to improve clinical symptoms of alcohol intoxication, including psychomotor agitation, depression, aggressiveness, and equilibrium disorders. There is also evidence that metadoxine has an effect on reducing craving for alcohol. Data from clinical studies also support an effect of metadoxine on reducing indices of liver cell necrosis and fat accumulation in alcoholic fatty liver.
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. Metadoxine, when given in an immediate release form in doses from 300 mg twice a day to 500 mg three times a day of up to 3 months, has been shown to improve biochemical indices of liver function as well as reduce ultrasonic evidence of fatty liver disease.
Metadoxine is a selective antagonist of the serotonin receptor subtype 5-HT2B and displays 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.
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.
Metadoxine is predominantly used as metadoxine immediate release formulation in developing nations for acute alcohol intoxication and chronic alcoholic liver disease. Alternate names include:
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