Expiration date: 03/2025

Pharmacological action

Pharmacological action - hypoglycemic, hypocholesterolemic, hepatoprotective

Pharmacodynamics

Thioctic acid (?-lipoic acid) is an endogenous antioxidant (free radicals), the body is formed from the oxidative decarboxylation of ?-ketoacids. As a coenzyme of mitochondrial multienzyme complexes involved in oxidative decarboxylation of pyruvic acid and ?-keto acids. Reduces the concentration of glucose in blood and increase of glycogen in the liver, as well as overcome insulin resistance. The nature of the biochemical action similar to the b vitamins. Involved in the regulation of lipid and carbohydrate metabolism, stimulates cholesterol metabolism, improves liver function. Has hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effect. Improves trophism of neurons.

Pharmacokinetics

At/in the introduction is 25-38 Cmax mcg/ml Tmax10–11 min, AUC is about 5 µg h/ml. Bioavailability of 30%.

Thioctic acid has a first pass effect through the liver. The formation of metabolites occurs as a result of oxidation of the side chain conjugation. Vd — 450 ml/kg of Thioctic acid and its metabolites are excreted by the kidneys (80-90%). T1/2 — 20-50 m. the Total plasma clearance of 10-15 ml/min.

Testimony

• diabetic neuropathy;
  
• alcoholic polyneuropathy.
  

Contraindications

• hypersensitivity to the drug;
  
• children up to age 18 years (efficacy and safety not established).
  

Application of pregnancy and breastfeeding

Contraindicated.

Side effects

At/in the introduction is very rarely possible convulsions; diplopia; petechiae in the mucous membranes, skin; thrombocytopathy; hemorrhagic rash (purpura), thrombophlebitis.

With the rapid introduction may increase intracranial pressure (feelings of heaviness in the head); difficulty breathing. These side effects are themselves.

Allergic reactions: urticaria, systemic allergic reactions (up to anaphylactic shock).

May develop hypoglycemia (in Association with improved glucose uptake).

Method of application and doses

In/in (drip infusion). The preparation is to be diluted in isotonic sodium chloride solution.

In severe forms of diabetic or alcoholic polyneuropathy should be administered 300-600 mg 1 time per day in/in drip infusions. The duration of infusion — 50 min. the product is recommended for 2-4 weeks.

You can then continue taking thioctic acid inside the dose 300-600 mg/day. The minimum period of treatment tablets — 3 months.