Espa-lipon (thioctic acid) coated tablets 600 mg. №30


Manufacturer: Germany

Treatment of diabetic polyneuropathy.



Espa-lipon Storage
active substance: thioctic acid (thioctic acid);

1 tablet contains thioctic acid 600 mg;

Excipients: lactose monohydrate, povidone, microcrystalline cellulose, powdered cellulose, highly dispersed silicon dioxide, precipitated silicon dioxide, sodium starch glycolate (type A), magnesium stearate, hypromellose, macrogol 6000, talc (yellow), tithium, titanium 104).

Espa-lipon Dosage form
Coated tablets.

Main physical and chemical properties: coated tablets, oblong, yellow with a notch for breaking.

Pharmacotherapeutic group
Drugs that affect the digestive system and metabolic processes. Thioctic acid.

Code ATX A16A X01.

Pharmacological properties


Thioctic acid is a substance that is formed in the body and acts as a coenzyme in the oxidative decarboxylation of α-keto acids. Hyperglycemia caused by diabetes leads to the deposition of glucose on the matrix proteins of blood vessels and the formation of end products of progressive glycosylation. This process leads to a decrease in endoneural blood flow and endoneural hypoxia / ischemia, associated with increased formation of free oxygen radicals that damage the nerve, as well as depletion of peripheral nerves such an antioxidant as glutathione. In 1995, a multicenter placebo-controlled study was conducted to examine the efficacy of thioctic acid for the symptomatic treatment of diabetic polyneuropathy, which provided data on the beneficial effects of thioctic acid on the studied symptoms such as paresthesias, burning, numbness, and pain.

Espa-lipon Pharmacokinetics.

Thioctic acid has a high first-pass effect in the liver. There are significant interpersonal differences in the systemic availability of thioctic acid. Biotransformation of thioctic acid occurs by oxidation of the side links and fusion. Excretion is carried out mainly by kidneys.

In humans, the plasma half-life is about 25 minutes, the total plasma clearance is 10-15 ml / min / kg. At the end of the 30-minute infusion of 600 mg, the determined plasma level is about 20 μg / ml. By radioactive labeling in animal studies (rats, dogs) was found predominant release of 80-90% of the drug in the form of metabolites. Also, people have only a small amount of unchanged substance excreted in the urine. Biotransformation occurs mainly by oxidative reduction of side units (beta-oxidation) and / or S-methylation of thiol groups.

Symptomatic treatment of diabetic polyneuropathy.

Hypersensitivity to thioctic acid or to any of the other components of the drug.

Interaction with other medicinal products and other forms of interaction
The effectiveness of cisplatin is reduced when used concomitantly with the drug. Thioctic acid is a complexing agent of metals and therefore, according to the basic principles of pharmacotherapy, it should not be used simultaneously with metal compounds (for example, with food additives containing iron or magnesium, with dairy products, because they contain calcium). If the total daily dose of the drug is used 30 minutes before breakfast, then supplements containing iron and magnesium should be used in the middle of the day or in the evening. With the use of thioctic acid in patients with diabetes may increase the hypoglycemic effect of insulin and oral antidiabetic drugs, so, especially at the initial stage of treatment, careful monitoring of blood sugar is recommended. In some cases, it may be necessary to reduce the dose of insulin or oral antidiabetic drugs to avoid the symptoms of hypoglycaemia.