Espa-lipon (thioctic acid) ampoules 600 mg. 24 ml. №5

Description

Espa-lipon 600 mg Espa-lipon Storage
active substance: thioctic acid (thioctic acid);

1 ampoule of the drug Espa-lipon®injection. 300 (12 ml) contains 377 mg of ethylenediamine salt of thioctic acid (equivalent to 300 mg of thioctic acid);

1 ampoule of the drug Espa-lipon®injection. 600 (24 ml) contains 755 mg of ethylenediamine salt of thioctic acid (equivalent to 600 mg of thioctic acid);

Espa-lipon Excipient: water for injections.

Espa-lipon 600 mg Dosage form
Solution for injection.

Main physical and chemical properties: clear solution of greenish-yellow color.

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

Code ATX A16A X01.

Pharmacological properties

Espa-lipon 600 mg Pharmacodynamics.

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.

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.

Indication
Treatment of diabetic polyneuropathy.

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

Interaction with other medicinal products and other forms of interaction
Thioctic acid reacts with metal ion complexes (eg, cisplastin), so the drug may reduce the effect of cisplastin.

With sugar molecules (for example, with a solution of levulose) thioctic acid forms sparingly soluble complex compounds.

Thioctic acid is a metal chelator, so it cannot be used with metals (eg iron, magnesium).

Thioctic acid may increase the antihypertensive effect of insulin and oral antidiabetic drugs, increasing the sensitivity of peripheral tissues to these drugs, and therefore it may be necessary to adjust the dose of insulin or oral antidiabetic drugs. For this reason, it is necessary to carefully monitor blood sugar, in particular at the initial stage of therapy.

Note.

Regular alcohol consumption is a significant risk factor for the development and progression of neuropathic syndromes and thus may affect the success of treatment with Espa-lipon® injection.300 / Espa-lipon® injection.600. Therefore, as a rule, patients with diabetic polyneuropathy are advised to avoid alcohol. This also applies to intervals when therapy is not performed.