Thioctic acid local edema reactions
Commercial proprietary name: Berlition® 300
International non-proprietary name or group name: thiocyic acid
Dosage form: concentrate for solution for infusion
Composition per one ampoule (12 ml):
Active substance: thioctic acid - 0.300 g.
Excipients: ethylenediamine 0.088 g, propylene glycol 0.932 g, water for injection 10.824 g.
Description: Transparent greenish-yellow solution.
Pharmacotherapeutic group: Metabolic means.
Thioktova (alpha-lipoic) acid - endogenousantioxidant direct (binds free radicals) and indirect action. It is a coenzyme of the reactions of decarboxylation of β-keto acids. It helps to reduce the concentration of glucose in the blood plasma and increase the concentration of glycogen in the liver, also reduces insulin resistance, participates in the regulation of carbohydrate and lipid metabolism, stimulates the exchange of cholesterol. Due to its antioxidant properties, thioctic acid protects cells from damaging them by decomposition products, reduces the formation of end products of progressive glycosylation of proteins in nerve cells in diabetes mellitus, improves microcirculation and endoneural blood flow, increases the physiological content of glutathione antioxidant. By contributing to a decrease in the concentration of glucose in the blood plasma, it affects the alternative metabolism of glucose in diabetes mellitus, reduces the accumulation of pathological metabolites in the form of polyols, and, thereby, reduces edema of the nervous tissue. Due to the participation in the metabolism of fats, thioctic acid increases the biosynthesis of phospholipids, in particular phosphoinositol, thereby improving the damaged structure of cell membranes; normalizes the energy exchange and the conduct of nerve impulses. Thioctic acid eliminates the toxic effect of alcohol metabolites (acetaldehyde, pyruvic acid), reduces the excess formation of molecules of free oxygen radicals, reduces endoneural hypoxia and ischemia, weakening manifestations of polyneuropathy in the form of paresthesias, burning sensations, pain and numbness of the extremities.
Thus, thioctic acid has antioxidant, neurotrophic, hypoglycemic action, improves lipid metabolism.
Application in the form of ethylenediamine salt allows to reduce the severity of possible side effects of thioctic acid.
With intravenous administration of 600 mg of thioctic acid, the maximum plasma concentration in 30 minutes is about 20 μg / ml.
Has the effect of "first passage" throughliver. The formation of metabolites occurs as a result of side chain oxidation and conjugation. Thioctic acid in the form of metabolites is excreted mainly by the kidneys (80-90%).
Half-life up to 25 min. The total plasma clearance is 10-15 ml / min / kg.
- Hypersensitivity to thiotide (? -lipoic) acid in history, hypersensitivity to other components of the drug;
- pregnancy, the period of breastfeeding (there is insufficient experience of the drug).
- age to 18 years (efficacy and safety of the drug are not established).
Application in pregnancy and during breastfeeding
Use of Berlition® 300 duringpregnancy is possible only if the intended benefit of therapy for the mother exceeds the potential risk to the fetus. In view of the lack of sufficient clinical experience in the use of Berlition® 300 during pregnancy and during breastfeeding, its use in appropriate categories of patients is not recommended.
Dosing and Administration
At the beginning of treatment, the preparation Berlition® 300 is prescribed intravenously drip in a daily dose of 300-600 mg (1-2 ampoules).
Before use, the contents of 1-2 ampoules (12-24 mldrug) diluted in 250 ml of 0.9% solution of sodium chloride and injected intravenously drip slowly, for at least 30 minutes. Since the active substance is sensitive to light, the infusion solution is prepared immediately prior to use. The prepared solution must be protected from exposure to light, for example, using aluminum foil. The light-shielded solution can be stored for about 6 hours.
The course of treatment is 2-4 weeks. Then they switch to maintenance therapy with Berlition® 300 (film-coated tablets) at a dose of 300-600 mg per day.
The duration of the course of treatment and the need for its recurrence is determined by the doctor.
Possible side effects with the use of the drug Berlition® 300 are given below on the descending frequency of occurrence: often (¼ 1/100,