Berlithion concentrate for solution for infusion 600ED (600mg)/24ml, 5 ampoules — Made in Germany — Free Delivery

Pharmacodynamics. Thioctic acid is a vitamin-like substance formed in the body and performs the function of a coenzyme during the oxidative decarboxylation of α-keto acids. Hyperglycemia caused by diabetes mellitus leads to the deposition of glucose on the matrix proteins of blood vessels and the formation of advanced glycosylation end products. this process leads to a decrease in endoneural blood flow and endoneural hypoxia / ischemia associated with an increased production of free oxygen radicals that damage the nerve, as well as depletion of an antioxidant such as glutathione in peripheral nerves.

In studies on rats, thioctic acid influenced the biochemical process caused by diabetes mellitus, which was triggered by streptozocin, decreased the formation of end products of progressive glycosylation, improved endoneural blood flow, increased the physiological content of glutathione, which acts in the nerve affected by the diabetic process similar to the action of an antioxidant relative to free oxygen radicals ... These effects suggest that thioctic acid may improve peripheral nerve function. This applies to sensory impairments that occur in polyneuropathy and can manifest as dysesthesias, paresthesias, such as pain, burning sensation, numbness or "creeping creeps." In 1995, a multicenter, placebo-controlled study was conducted to investigate the efficacy of thioctic acid for the symptomatic treatment of diabetic polyneuropathy, in which data were obtained on the beneficial effects of thioctic acid on such studied symptoms as paresthesias, burning sensation, numbness and pain.

Pharmacokinetics. Thioctic acid is highly susceptible to the effect of the primary passage through the liver. Systemic bioavailability is characterized by significant individual variations. Biotransformation of thioctic acid occurs by side chain oxidation and conjugation and is excreted mainly by the kidneys. T½ of thioctic acid in humans is about 25 minutes, and the total clearance in blood plasma is 10-15 ml / min / kg. After a 30-minute infusion of 600 mg of thioctic acid, its plasma concentration is about 20 μg / ml. In experiments on animals (rats, dogs), using a radioactive label, it was possible to reveal the predominant excretion by the kidneys (80-90%), namely, in the form of metabolites. In humans, there is also only a small amount of excreted intact substance in the urine. Metabolism occurs mainly by side chain oxidation (β-oxidation) and / or by S-methylation of the corresponding thiols.

Thioctic acid interacts in vitro with ionic metal complexes (for example, with cisplatin).

Thioctic acid forms poorly soluble complex compounds with sugar molecules.

Paresthesia in diabetic polyneuropathy.

Doses. In case of intense paresthesias caused by diabetic polyneuropathy, it is recommended to intravenously administer a concentrate for an infusion solution at a dose of 12 ml (1 ampoule of Berlithion 300 U) to 24 ml (2 ampoules of Berlithion 300 U or 1 ampoule of Berlithion 600 U) per day , which corresponds to 300-600 mg of thioctic acid per day.

Mode of application. After dilution, the concentrate for the preparation of the solution for infusion is used intravenously for 2-4 weeks at the initial stage of treatment. The contents of 1 or 2 ampoules of the preparation Berlithion 300 U or 1 ampoule of Berlithion 600 U are diluted in 250 ml of 0.9% sodium chloride solution and administered intravenously, the duration of the infusion should be at least 30 minutes. Due to the sensitivity of the active substance to light, an infusion solution is prepared immediately before administration and protected from light, for example, using aluminum foil. The prepared solution for infusion can be stored for 6 hours, provided it is protected from light.

For further therapy, oral forms of thioctic acid are indicated at a dose of 300–600 mg / day.