

Thioctic acid (alpha-lipoic acid) - an endogenous antioxidant (binds free radicals), is formed in the body during the oxidative decarboxylation of alpha keto acids. As a coenzyme, mitochondrial multienzyme complexes are involved in the oxidative decarboxylation of pyruvic acid and alpha-keto acids.
By the nature of the biochemical action is similar to the B vitamins. It has a hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effect. Helps reduce blood glucose and increase glycogen content in the liver, as well as reduce insulin resistance.
Participates in the regulation of lipid and carbohydrate metabolism, stimulates the exchange of cholesterol, improves liver function. Improves trophism of neurons. The use of the megoulamine salt of thioctic acid (which has a neutral reaction) makes it possible to reduce the severity of side reactions.
Pharmacokinetics
The time to reach maximum concentration is 10-11 minutes. The area under the concentration-time curve is about 5 μg × h / ml.
Bioavailability - 30%. It has the effect of "first pass" through the liver. Metabolized in the liver by side chain oxidation and conjugation. The volume of distribution is about 450 ml / kg. Total plasma clearance - 10-15 ml / min. Thioctic acid and its metabolites are excreted by the kidneys (80-90%). The half-life is 20-50 minutes.
Diabetic and alcoholic neuropathy.
1 ml of solution contains:
Active substance: thioctic acid (alpha lipoic acid) 12.00 mg;
Excipients: meglumine (N-methyl-D-glucamine), macrogol (polyethylene glycol 400), povidone (collidon® 17 РF or plasdon C-15), water for injection.
Thioctic acid is marketed under different brands and generic names, and comes in different dosage forms:
Brand name | Manufacturer | Country | Dosage form |
---|---|---|---|
Tiolepta | Canonpharma | Russia | solution |
Espa-lipon | Esparma | Germany | ampoules |
Thiolipon | Biosynthesis | Russia | pills |
Octolipen | Pharmstandard | Russia | pills |
Berlition | Berlin-Chemie/Menarini | Germany | ampoules |
Tiolepta | Canonpharma | Russia | pills |
Thioctacid BV | Meda Pharma GmbH & Co. KG | Switzerland | pills |
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The preparation is intended for preparation of solution for infusions after preliminary cultivation in isotonic solution of sodium chloride.
Severe forms of diabetic or alcoholic neuropathy
Once a day in the form of intravenous drip infusions 24 ml of solution in 250 ml of isotonic solution of sodium chloride (which corresponds to 600 mg of alpha-lipoic acid per day). The drug is recommended to be used within 2-4 weeks. Solutions for infusion should be administered within 50 minutes. Prepared solutions must be stored in a dark place and used for a maximum of 6 hours after preparation.
Next, you should switch to maintenance therapy in the form of pills at a dose of 400-600 mg per day. The minimum duration of treatment with pills is 3 months.
Allergic reactions are possible: urticaria, systemic allergic reactions (up to the development of anaphylactic shock). Perhaps the development of hypoglycemia (due to improved glucose uptake). If ingestion may be dyspeptic symptoms, including nausea, heartburn, vomiting.
When administered intravenously, seizures are very rare; diplopia; point hemorrhages in mucous membranes, skin; thrombocytopathy; hemorrhagic rash (purpura), thrombophlebitis.
With the rapid introduction may increase intracranial pressure (the emergence of a feeling of heaviness in the head); difficulty breathing.
Thioctic (alpha-lipoic) acid forms difficult soluble complex compounds with sugar molecules (for example, levulose solution), therefore, it is incompatible with glucose solution, Ringer's solution, and also with compounds (including their solutions) that interact with disulfide and SH – groups.
Thioctic (alpha-lipoic) acid (as an infusion solution) reduces the effect of cisplatin.
The possibility of using Espa-lipon during pregnancy is determined by the attending physician. Breastfeeding should be discontinued at the time of treatment (no data are available on whether alpha-lipoic acid is excreted in breast milk).
In patients with diabetes mellitus, especially at the beginning of treatment, frequent monitoring of glucose concentration in the blood is necessary. In some cases, a reduction in the dose of hypoglycemic agents is required.
During treatment, it is necessary to strictly abstain from alcohol, since the therapeutic effect of thioctic (alpha-lipoic) acid is weakened when exposed to alcohol.
Symptoms: headache, nausea, vomiting.
Treatment: symptomatic. There is no specific antidote.
Studies and clinical trials of Thioctic acid (Click to expand)