Metadoxil, 500 mg.

Active substance:

methadoxine (pyridoxine L-2 pyrrolidone 5-carboxylate) 500 mg;

Excipients:

MCC;

magnesium stearate

Metadoxyl - detoxification, hepatoprotective, anti-alcohol drug.

Pharmacodynamics

The hepatoprotective effect of the active substance is due to the membrane-stabilizing effect and is based on the ability to restore the ratio of saturated and unsaturated free fatty acids. As a result of this action, the resistance of hepatocytes to the action of lipid peroxidation, which occurs when exposed to various toxic agents, is increased.

The detoxifying effect of metadoxine is due to the activation of liver enzymes involved in the metabolism of ethanol - alcohol dehydrogenase and acetaldehyde dehydrogenase, which accelerates the process of elimination of ethanol and acetaldehyde from the body, and therefore, their toxic effect is reduced.

Metadoxine prevents the accumulation of triglycerides in hepatocytes, and also prevents the formation of fibronectin and collagen, which significantly slows down the formation of liver cirrhosis.

The drug lowers the mental and somatic manifestations of a hangover syndrome, reduces the time to relieve withdrawal symptoms.

Metadoxine activates cholinergic and GABAergic neurotransmitter systems, improves thinking and short memory functions, and prevents the occurrence of motor excitation, which is caused by ethanol.

Metadoxine has a non-specific antidepressant and anxiolytic effect, reduces the craving for alcohol.

Pharmacokinetics

It is quickly absorbed from the gastrointestinal tract, has a high bioavailability (60–80%). Binding to plasma proteins - 50%. It is metabolized in the liver to active metabolites - pyridine and pyrrolidone carboxylate. T _1/2  when administered orally or parenterally is 40-60 minutes. 45-50% of the drug is excreted in the urine for 24 hours, 35-50% of the drug is excreted in the feces for 96 hours.

• prevention of liver diseases, alcohol etiology;
• acute alcohol intoxication;
• chronic alcoholism;
• alcohol withdrawal syndrome.

Metadoxil Contraindicated in pregnancy and lactation.

• hypersensitivity to any component of the drug;
• pregnancy;
• lactation period.

With caution: use with caution in Parkinson's disease if levodopa is used at the same time, because methadoxine reduces the effectiveness of the drug.

In the ampoules of the solution for injection contains sodium metabisulfite. This substance can cause allergic reactions or increased asthma attacks in susceptible people, especially those with asthma.

Allergic reactions. In patients suffering from bronchial asthma, the development of bronchospasm with the use of an injection is possible.

When combined, reduces the effectiveness of levodopa.

Acute alcohol intoxication: 300–600 mg (5–10 ml) iv or 300–900 mg (5–15 ml) iv, depending on the degree of intoxication.

With the on / in the introduction, the required dose of the drug is diluted in 500 ml of isotonic sodium chloride solution or 5% dextrose (glucose) solution and administered dropwise for 1.5 hours.

Combination therapy of liver diseases and chronic alcoholism: inside: 1 tab. 2 times a day (1000 mg) for 15-30 minutes before a meal, the dose can be increased to 3 tablets. (1500 mg) per day. The course of therapy should be at least 90 days.

Alcohol withdrawal syndrome: 900 mg (15 ml) as an intravenous infusion (see above) 1 time per day for 3–7 days, depending on the patient’s condition.

Currently, cases of an overdose of Metadoxil have not been reported.

With caution, a drug should be prescribed for Parkinson's disease if levodopa is used at the same time, because metadoxine reduces the effectiveness of the latter.

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