Berlition 300 U concentrate for prig. solution for infusion 25mg / ml, 12ml No. 5

Diabetic and alcoholic polyneuropathy, steatohepatitis of various etiologies, fatty degeneration of the liver, chronic intoxication.

I / O, inside. In severe forms of polyneuropathy IV, 12-24 ml (300-600 mg of alpha-lipoic acid) per day for 2-4 weeks. To do this, 1Ц2 ampoules of the drug are diluted in 250 ml of physiological 0.9% sodium chloride solution and injected drip for about 30 minutes. In the future, they switch to maintenance therapy with Berlition 300 in the form of tablets at a dose of 300 mg per day.

For the treatment of polyneuropathy - 1 table. 1-2 times a day (300-600 mg of alpha lipoic acid).

Active ingredient: thioctic acid - 0.300 g.

Excipients: ethylenediamine - 0.088 g, propylene glycol - 0.932 g, water for injection - 10.824 g.

• Hypersensitivity

• pregnancy, breastfeeding.

• Cannot be prescribed to children and adolescents (due to the lack of clinical experience of using this drug in them).

Pharmacodynamics

Thioctic (alpha lipoic) acid is an endogenous antioxidant of direct (binds free radicals) and indirect action. It is a coenzyme of reactions of decarboxylation of a-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, and stimulates cholesterol metabolism. Due to its antioxidant properties, thioctic acid protects cells from damage by their decay products, reduces the formation of end products of progressive glycosylation of proteins in nerve cells in diabetes mellitus, improves microcirculation and endoneural blood flow, and increases the physiological content of the antioxidant glutathione. By helping to reduce the concentration of glucose in the blood plasma,affects the alternative glucose metabolism in diabetes mellitus, reduces the accumulation of pathological metabolites in the form of polyols, and thereby reduces the edema of the nervous tissue. Due to its participation in the metabolism of fats, thioctic acid increases the biosynthesis of phospholipids, in particular, phosphoinoisite, thereby improving the damaged structure of cell membranes; normalizes energy metabolism and conduction of nerve impulses. Thioctic acid eliminates the toxic effect of alcohol metabolites (acetaldehyde, pyruvic acid), reduces the excessive formation of free oxygen radicals, reduces endoneural hypoxia and ischemia, weakening the manifestations of polyneuropathy in the form of paresthesias, burning sensations, pain and numbness of the extremities. Thus, thioctic acid has an antioxidant, neurotrophic,hypoglycemic effect, improves lipid metabolism. Application in the form of ethylenediamine salt can reduce the severity of possible side effects of thioctic acid.

Pharmokinetics

With the intravenous administration of 600 mg of thioctic acid, the maximum concentration in the blood plasma after 30 minutes is about 20 ?g / ml. Has a 'first pass' effect through the liver. 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%). The half-life is up to 25 minutes. The total plasma clearance is 10-15 ml / min / kg.

Side effects

From the nervous system: Very rarely: change or violation of taste, diplopia, convulsions.

From the hemostatic system: Very rarely: purpura, thrombocytopathy.

From the side of metabolism: Very rarely: a decrease in the level of glucose in the blood plasma (due to an improvement in the absorption of glucose). Complaints indicative of a hypoglycemic state have been reported, such as dizziness, sweating, headache, and blurred vision.

From the immune system: Very rarely: allergic reactions such as skin rash, urticaria (urticaria), itching, in rare cases - anaphylactic shock.

Local reactions: Very rare: burning sensation at the injection site

Others: with rapid intravenous administration, spontaneous increases in intracranial pressure (a feeling of heaviness in the head) and difficulty in breathing were observed.

Special conditions

In patients with diabetes mellitus taking insulin or hypoglycemic drugs for oral administration, constant monitoring of plasma glucose concentration is necessary, especially at the initial stage of therapy with BerlitionЃ300. In some cases, it may be necessary to reduce the dose of insulin or oral hypoglycemic drugs in order to avoid the development of hypoglycemia. With parenteral administration, hypersensitivity reactions may occur. If symptoms such as itching, nausea, malaise appear, treatment with BerlitionЃ 300 should be stopped immediately. Alcohol intake reduces the effectiveness of treatment with BerlitionЃ 300, therefore, patients during therapy with BerlitionЃ 300 should refrain from drinking alcohol throughout the course of treatment, and, if possible,in between courses. The prepared solution of BerlitionЃ 300 should be protected from light. The effect of the drug on the ability to drive vehicles and mechanisms: The effect of BerlitionЃ 300 on the ability to drive vehicles and control mechanisms has not been specifically studied, therefore, during the period of treatment with BerlitionЃ 300, care should be taken when driving vehicles and engaging in potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions.The effect of BerlitionЃ 300 on the ability to drive vehicles and control mechanisms has not been specifically studied, therefore, during the period of treatment with BerlitionЃ 300, care should be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.The effect of BerlitionЃ 300 on the ability to drive vehicles and control mechanisms has not been specifically studied, therefore, during the period of treatment with BerlitionЃ 300, care should be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Drug interactions

Due to the fact that thioctic acid is capable of forming chelate complexes with metals, co-administration with iron preparations should be avoided. The simultaneous use of the drug BerlitionЃ 300 with cisplatin reduces the effectiveness of the latter. Thioctic acid forms poorly soluble complex compounds with sugar molecules. BerlitionЃ 300 is incompatible with solutions of glucose, dextrose, fructose, Ringer, as well as solutions that react with SH-groups or disulfide bonds. The drug BerlitionЃ 300 enhances the hypoglycemic effect of insulin and hypoglycemic drugs for oral administration when used together. Ethanol reduces the therapeutic efficacy of BerlitionЃ 300.