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Thioctic acid

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Clinical Pharmacology

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.


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 nameManufacturerCountryDosage 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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Thioctic acid

Dosage and Administration

TheraFlu LAR is used topically.

Solution in the form of a spray: spray in the mouth, holding the can vertically.

For adults - 4 sprays (approximately 0.5 ml) 3–6 times a day.

Children aged 4 and over - 1 to 2–3 sprays 3–6 times per day.

The duration of treatment is not more than 5 days. If there is relief of symptoms within 5 days of therapy, the patient should consult a doctor.

Adverse reactions

Local irritation may develop; when applied for more than 2 weeks - reversible brown color of the tongue and teeth.

  • Hypersensitivity to lidocaine or ammonia compounds;
  • I trimester of pregnancy;
  • lactation period (breastfeeding);
  • children's age (up to 4 years).

Special instructions

While using Theraflu LAR, alcohol should be avoided.

  • Brand name: Theraflu LAR
  • Active ingredient: Benzalkoniya chloride, Lidocaine
  • Dosage form: Topical spray
  • Manufacturer: Novartis
  • Country of Origin: Switzerland

Studies and clinical trials of Thioctic acid (Click to expand)

  1. Thioctic acid in wheat flour
  2. Lipoic acid (thioctic acid) analogs, tryptophan analogs, and urea do not interfere with the assay of biotin and biotin metabolites by high-performance liquid chromatography/avidin-binding assay
  3. Direct application strategy to immobilise a thioctic acid self-assembled monolayer on a gold electrode
  4. Electrochemical detection of lead ions via the covalent attachment of human angiotensin I to mercaptopropionic acid and thioctic acid self-assembled monolayers
  5. Comparative Treatment of α-Amanitin Poisoning With N-Acetylcysteine, Benzylpenicillin, Cimetidine, Thioctic Acid, and Silybin in a Murine Model
  6. In response to Tong TC, et al. Comparative treatment of alpha-amanitin poisoning with N-acetylcysteine, benzylpenicillin, cimetidine, thioctic acid, and silybin in a murine model
  7. A comparative study of capacitive immunosensors based on self-assembled monolayers formed from thiourea, thioctic acid, and 3-mercaptopropionic acid
  8. Potential control characteristics of short-chain thiols of thioctic acid and mercaptohexanol self-assembled on gold
  9. Electron transfer studies through mixed self-assembled monolayers of thiophenol and thioctic acid
  10. Voltammetry of immobilized cytochrome c on novel binary self-assembled monolayers of thioctic acid and thioctic amide modified gold electrodes
  11. Thioctic acid modification of oligonucleotides using an H-phosphonate
  12. Studies on the effect of solvents on self-assembly of thioctic acid and Mercaptohexanol on gold
  13. In vivo determination of the monoamine neurotransmitters in rat brain by liquid chromatography with a thioctic acid/iridium oxide–palladium modified electrode
  14. Characterization and gas chromatographic determination of active principles of biological interest in pharmaceutical products (gastric mucoprotein and thioctic acid)
  15. Nature of immobilized antibody layers linked to thioctic acid treated gold surfaces
  16. Burning mouth syndrome (BMS): double blind controlled study of alpha-lipoic acid (thioctic acid) therapy
  17. Lack of interaction between thioctic acid, glibenclamide and acarbose
  18. Effects of 3-week oral treatment with the antioxidant thioctic acid (α-lipoic acid) in symptomatic diabetic polyneuropathy
  19. Treatment of experimental tumours by thioctic acid
  20. Lipoic (thioctic) acid increases brain energy availability and skeletal muscle performance as shown by in vivo31P-MRS in a patient with mitochondrial cytopathy
  21. Immobilization of proteins on gold coated porous membranes via an activated self-assembled monolayer of thioctic acid
  22. Thioctic acid does not restore glutathione levels or protect against the potentiation of 6-hydroxydopamine toxicity induced by glutathione depletion in rat brain
  23. Influence of food intake on the bioavailability of thioctic acid enantiomers

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