Usage
Metadoxine is prescribed for the treatment of acute and chronic alcohol intoxication and alcoholic fatty liver disease. It acts as a hepatoprotective agent, safeguarding the liver from alcohol-induced damage. It also aids in managing alcohol dependence by reducing withdrawal symptoms. Its pharmacological classification is detoxification agent. Metadoxine accelerates the metabolism of ethanol, diminishing its toxic effects, and protects liver cells by antagonizing lipid peroxidation and restoring liver function.
Alternate Names
An alternate name for Metadoxine is Metadoxil. Metadoxil is also a common brand name.
How It Works
Pharmacodynamics: Metadoxine increases the release of GABA and acetylcholine, neurotransmitters involved in alcohol intoxication. It also counteracts lipid peroxidation in liver cells, thus mitigating alcohol-induced liver damage and reducing fatty liver in chronic hepatitis. This promotes faster recovery from alcohol intoxication and protects liver cells from damage. It improves ethanol metabolism, reducing plasma ethanol levels during alcohol intake, leading to improved cognitive function. It also helps in reducing psychological symptoms like aggression and mood disturbances associated with alcohol abuse.
Pharmacokinetics: Metadoxine is available in oral, intramuscular (IM), and intravenous (IV) forms. The oral form is typically taken before meals. It is primarily metabolized in the liver and excreted through the kidneys. Specific details about its absorption, distribution, and half-life are not readily available in current research.
Mode of Action: Metadoxine works by increasing the activity of enzymes involved in alcohol metabolism, particularly alcohol dehydrogenase and aldehyde dehydrogenase. It also inhibits the formation of free radicals and lipid peroxidation, both of which contribute to liver damage. In addition, it may block the differentiation of preadipocytes, reducing the accumulation of fat in the liver.
Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: Metadoxine has a unique mechanism of action involving selective antagonism of the serotonin receptor subtype 5-HT2B. By binding to this receptor, it may exert some of its therapeutic effects. The interaction details are not precisely understood but may relate to influencing ethanol’s effects on the central nervous system.
Dosage
Standard Dosage
Adults:
- Oral: 500-1000 mg/day for acute alcohol intoxication; 1000 mg/day for alcoholic fatty liver disease.
- IM/IV: 300-600 mg/day for acute alcohol intoxication; 300 mg/day for alcoholic fatty liver disease.
Children:
Metadoxine is generally not recommended for children due to limited safety and efficacy data.
Special Cases:
- Elderly Patients: Dosage adjustments are not typically required.
- Patients with Renal Impairment: Exercise caution; dosage adjustments may be necessary.
- Patients with Hepatic Dysfunction: For alcoholic liver disease, standard dosages can be used. Avoid in severe liver failure.
- Patients with Comorbid Conditions: Patients with Parkinson’s disease taking levodopa should be monitored as metadoxine might reduce levodopa’s efficacy.
Clinical Use Cases
Dosage guidelines for specific clinical use cases like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations haven’t been definitively established.
Dosage Adjustments
Dose modifications should be considered for patients with renal or hepatic impairment. Always consult a healthcare professional before adjusting the dose.
Side Effects
Common Side Effects:
Nausea, vomiting, diarrhea, headache, dizziness, fatigue, skin rash, itching.
Rare but Serious Side Effects:
Hypersensitivity reactions, peripheral neuropathy, angioedema.
Long-Term Effects:
The long-term effects of Metadoxine are not well-established in the current literature.
Adverse Drug Reactions (ADR):
Allergic reactions, including skin rash, itching, and angioedema.
Contraindications
Hypersensitivity to metadoxine, pyridoxine, or pidolic acid. Severe liver impairment. Pregnancy and lactation.
Drug Interactions
Metadoxine may interact with levodopa, reducing its effectiveness. It may also interact with sedative agents (e.g., benzodiazepines) and opioids. Alcohol should be avoided as it may exacerbate liver damage.
Pregnancy and Breastfeeding
Metadoxine is contraindicated during pregnancy and breastfeeding due to potential risks to the fetus and neonate.
Drug Profile Summary
- Mechanism of Action: Enhances alcohol elimination, protects liver cells, modulates neurotransmitters.
- Side Effects: Nausea, vomiting, diarrhea, headache, dizziness, skin rash, itching, rare allergic reactions.
- Contraindications: Hypersensitivity, severe liver impairment, pregnancy, lactation.
- Drug Interactions: Levodopa, sedatives, opioids, alcohol.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Varies based on condition and administration route (see detailed section).
- Monitoring Parameters: Liver function tests, neurological status, blood glucose levels (for diabetics).
Popular Combinations
Metadoxine is sometimes combined with silymarin for enhanced hepatoprotective effects. The combination may also include L-ornithine L-aspartate, pyridoxine, and folic acid.
Precautions
- General Precautions: Evaluate for allergies, assess liver and kidney function, monitor for side effects.
- Specific Populations: Contraindicated in pregnant and breastfeeding women. Not generally recommended for children. Use with caution in patients with renal impairment.
- Lifestyle Considerations: Avoid alcohol.
FAQs (Frequently Asked Questions)
A: The dosage depends on the condition and administration route. For adults, oral dosages range from 500-1000 mg/day for acute alcohol intoxication and 1000 mg/day for alcoholic fatty liver disease. IM/IV doses are 300-600 mg/day and 300 mg/day, respectively. Pediatric dosage is not established.
A: The primary use is to treat acute and chronic alcohol intoxication and alcoholic fatty liver disease.
A: Common side effects include nausea, vomiting, diarrhea, headache, dizziness, fatigue, skin rash, and itching.
A: No, it is contraindicated in both pregnancy and breastfeeding.
A: Yes, it can interact with Levodopa, sedatives, and opioids. It’s also important to avoid alcohol.
A: It enhances alcohol elimination, antagonizes lipid peroxidation, and modulates neurotransmitters related to alcohol intoxication.
A: Yes, contraindications include hypersensitivity, severe liver impairment, pregnancy, and breastfeeding.
A: Assess for allergies, evaluate liver and kidney function, monitor for adverse reactions, and advise patients to avoid alcohol. Use with caution in patients with renal impairment.
A: Use caution in patients with Parkinson’s disease taking levodopa as Metadoxine may reduce its efficacy. Monitor these patients closely.
This information is current as of February 16, 2025, and might change with future research.
