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What Is Metadoxine ? – Dosage, Pregnancy Category

Last updated: February 7, 2026 Medically reviewed by: RxHarun Orthopedic Specialist Doctor Reading time: 5 min read

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-HT2B 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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Dosage of Metadoxine

  • 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.

Acute alcohol intoxication

  • 0.5-1 g/day.

Alcoholic fatty liver;

  • Adjunct in acute and chronic liver diseases 1 g/day. IV/IM

Acute alcohol intoxication

  • 300-600 mg/day. Alcoholic fatty liver; Adjunct in acute and chronic liver diseases 300 mg/day.

Acute alcohol intoxication

  • Adult: 500-1000 mg daily.

Alcoholic fatty liver, Supportive treatment of acute and chronic liver diseases

  • Adult: 1000 mg daily.

Acute alcohol intoxication

  • Adult: 300-600 mg daily IM/IV.

Alcoholic fatty liver, Supportive treatment of acute and chronic liver diseases

  • Adult: 300 mg daily IM/IV.

Missed Dose

  • Oral Form – The missed dose should be taken as soon as possible. It is advisable to skip the missed dose if it is already time for your next scheduled dose. Do not use extra medicine to make up for the missed dose.
  • Injection – Since this medicine is administered in the hospital/clinic setting by a qualified healthcare professional, the likelihood of a missed dose is very low. If you miss a scheduled appointment for a dose of this medicine, contact your doctor for further instructions.

Overdose

  • Oral Form – Seek emergency medical treatment or contact the doctor in case of an overdose. Injection: Since this medicine is administered in the hospital/clinic setting by a qualified healthcare professional, the likelihood of an overdose is very low. However, emergency medical treatment will be initiated by the doctor if an overdose is suspected.

Side Effects of Metadoxine

Major & minor side effects for Metadoxine

Interactions of Metadoxine

  • All drugs interact differently from person to person. You should check all the possible interactions with your doctor before starting any medicine.

Interaction with Alcohol

  • Interaction with alcohol is unknown. It is advisable to consult your doctor before consumption.

Instructions

  • Interaction with alcohol is unknown. It is advisable to consult your doctor before consumption.

Interaction with Medicine

Levodopa

  • Disease interactions

Disease

  • Information not available.
Food interactions
  • Information not available.
Lab interactions
  • Information not available. This is not an exhaustive list of possible drug interactions. You should consult your doctor about all the possible interactions of the drugs you’re taking.

Pregnancy Category of Metadoxine

  • Information not available

References

Frequently Asked Questions

Is this article a replacement for a doctor?

No. It is educational content only. Patients should consult a qualified clinician for diagnosis and treatment.

When should I seek urgent care?

Seek urgent care for severe symptoms, rapidly worsening condition, breathing difficulty, severe pain, neurological changes, or any emergency warning sign.

References

Add references, clinical guidelines, textbooks, journal articles, or trusted medical sources here. You can edit this area later with a custom field named _rx_references.

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Written by Dr. Harun Ar Rashid, MD - Arthritis, Bones, Joints Pain, Trauma, and Internal Medicine Specialist

Dr. Md. Harun Ar Rashid, MPH, MD, PhD, is a highly respected medical specialist celebrated for his exceptional clinical expertise and unwavering commitment to patient care. With advanced qualifications including MPH, MD, and PhD, he integrates cutting-edge research with a compassionate approach to medicine, ensuring that every patient receives personalized and effective treatment. His extensive training and hands-on experience enable him to diagnose complex conditions accurately and develop innovative treatment strategies tailored to individual needs. In addition to his clinical practice, Dr. Harun Ar Rashid is dedicated to medical education and research, writing and inventory creative thinking, innovative idea, critical care managementing make in his community to outreach, often participating in initiatives that promote health awareness and advance medical knowledge. His career is a testament to the high standards represented by his credentials, and he continues to contribute significantly to his field, driving improvements in both patient outcomes and healthcare practices. Born and educated in Bangladesh, Dr. Rashid earned his BPT from the University of Dhaka before pursuing postgraduate training internationally. He completed his MD in Internal Medicine at King’s College London, where he developed a special interest in inflammatory arthritis and metabolic bone disease. He then undertook a PhD in Orthopedic Science at the University of Oxford, conducting pioneering research on cytokine signaling pathways in rheumatoid arthritis. Following his doctoral studies, Dr. Rashid returned to clinical work with a fellowship in interventional pain management at the Rx University School of Medicine, refining his skills in image-guided joint injections and minimally invasive pain-relief techniques.