Berlition 600ED concentrate for the preparation of solution for infusion 24ml No. 5 ampoules

Composition and release form

in brown glass ampoules of 12 ml; in a cardboard box there are 5, 10 or 20 ampoules.

in a blister pack 10 pcs.; There are 3, 6 or 10 packs in a cardboard box.

pharmachologic effect

Pharmacological action - hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic.

As a coenzyme of mitochondrial multienzyme complexes, it participates in the oxidative decarboxylation of pyruvic acid and alpha-keto acids. Helps reduce blood glucose and increase glycogen content in the liver, as well as overcome insulin resistance. By the nature of its biochemical action it is close to B vitamins. Participates in the regulation of lipid and carbohydrate metabolism, stimulates cholesterol metabolism, and improves liver function. The use of trometamol salt of thioctic acid (which has a neutral reaction) in solutions for intravenous administration can reduce the severity of adverse reactions.

Berlition 600ED concentrate for the preparation of solution for infusion 24ml No. 5 ampoules

Trade name: Berlition 600

International generic name: Thioctic acid

Release form and packaging: Concentrate for the preparation of solution for infusion. Concentrate for the preparation of a solution for infusion, 24 ml in dark glass ampoules, 5 ampoules each, placed in a cardboard box.

Pharmacological action: Pharmacodynamics Thioctic (β-lipoic) acid is an endogenous antioxidant (binds free radicals), formed in the body during the oxidative decarboxylation of β-keto acids. As a coenzyme of mitochondrial multienzyme complexes, it participates in the oxidative carboxylation of pyruvic acid and β-keto acids. Helps reduce blood glucose and increase glycogen content in the liver, as well as overcome insulin resistance. By the nature of its biochemical action it is close to B vitamins. Participates in the regulation of lipid and carbohydrate metabolism, stimulates cholesterol metabolism, and improves liver function. It has hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effects. The use of ethylenediamine salt of thioctic acid in solutions for intravenous administration (which has a neutral reaction) can reduce the severity of adverse reactions.

Pharmacokinetics Absorption and distribution. With intravenous administration, Cmax is 25-38 mcg/ml and is achieved after 10-11 minutes, AUC is about 5 mcg x h/ml. Vd is about 450 ml/kg. Metabolism and excretion. Has a “first pass” effect through the liver. The formation of metabolites occurs as a result of side chain oxidation and conjugation. Thioctic acid and its metabolites are excreted in the urine (80-90%).

Special instructions: The results of clinical studies in recent years have shown the high effectiveness of the use of thioctic (a-lipoic) acid for patients with type 2 diabetes mellitus with cardiovascular manifestations of diabetic neuropathy. The therapeutic effect of Berlition in this group of patients may be the result of the drug’s effect on the autonomic nervous system, in particular by increasing the speed of wave propagation in visceral parasympathetic and sympathetic fibers. Use in pediatrics Berlition should not be prescribed to children and adolescents due to the lack of clinical experience with the drug in this category of patients.

Composition: 1 ml (1 ampoule) contains: Active substance: ethylenediamine salt of thioctic (?-lipoic) acid 64.66 mg (776 mg), which corresponds to the content of thioctic (?-lipoic) acid 50 mg (600 mg). Excipients: propylene glycol, ethylenediamine, water for injection.

Method of administration and dosage: In severe forms of polyneuropathy, at the beginning of treatment the drug is prescribed intravenously at 300-600 mg (respectively 12-24 ml)/day for 2-4 weeks. Subsequently, they switch to maintenance therapy and prescribe tablets of 300 mg (1 tablet) 1 time/day. When administered intramuscularly, the dose administered at one injection site should not exceed 50 mg (2 ml). IM administration of the drug in high doses must be carried out in the form of several injections (2 ml for each injection site).

Side effects: From the central nervous system: very rarely - convulsions, diplopia; With rapid intravenous administration, there may be a feeling of heaviness in the head (increased intracranial pressure) and difficulty breathing, which go away on their own. From the blood coagulation system: very rarely - petechiae on the skin and mucous membranes, thrombocytopathy, hemorrhagic rash (purpura), thrombophlebitis. Metabolism: possible - hypoglycemia (due to improved glucose absorption). Allergic reactions: possible - urticaria, systemic allergic reactions up to anaphylactic shock. Local reactions: possible - burning at the injection site.

Drug interactions: In vitro, thioctic (a-lipoic) acid reacts with complexes containing metal ions (for example, cisplatin). Therefore, when taken simultaneously with cisplatin, the effect of Berlition may be weakened. When used simultaneously, ethanol and its metabolites may weaken the effect of Berlition. Berlition enhances the hypoglycemic effect of insulin and oral hypoglycemic agents. Pharmaceutical interaction. Thioctic (a-lipoic) acid forms sparingly soluble complex compounds with glucose molecules (including levulose solutions). Berlition is incompatible with glucose solutions, Ringer's solution, and solutions known to react with SH groups or disulfide bridges.

Overdose: Symptoms: nausea, vomiting, headache. In severe cases: psychomotor agitation or clouding of consciousness, generalized convulsions, severe acid-base imbalance, lactic acidosis, hypoglycemia (up to the development of coma), acute necrosis of skeletal muscles, disseminated intravascular coagulation syndrome, hemolysis, suppression of bone marrow activity, multiple organ failure. Treatment: If thioctic acid intoxication is suspected (for example, administration of more than 80 mg of thioctic acid per 1 kg of body weight), emergency hospitalization and immediate application of measures in accordance with the general principles adopted for accidental poisoning are recommended. Therapy is symptomatic. Treatment of generalized seizures, lactic acidosis and other life-threatening consequences of intoxication should be carried out in accordance with the principles of modern intensive care. There is no specific antidote. Hemodialysis, hemoperfusion, or filtration methods with forced removal of thioctic acid are not effective.

Storage conditions: Store in a dry, cool place, protected from light.

Shelf life: 3 years.

Conditions for dispensing from pharmacies: Dispensed with a doctor's prescription

Pharmacokinetics

When taken orally, it is quickly and completely absorbed from the gastrointestinal tract (taken with food reduces absorption). Time to reach Cmax is 40–60 minutes. Bioavailability - 30%. Has a “first pass” effect through the liver. The formation of metabolites occurs as a result of side chain oxidation and conjugation. Volume of distribution is about 450 ml/kg. The main metabolic pathways are oxidation and conjugation. Thioctic acid and its metabolites are excreted by the kidneys (80–90%). T1/2 - 20–50 min. Total plasma Cl - 10–15 ml/min.

Berlition 300 mg 30 pcs. film-coated tablets

pharmachologic effect

Metabolic agent.

Composition and release form Berlition 300 mg 30 pcs. film-coated tablets

Tablets - 1 tablet:

• Active ingredient: thioctic acid - 300 mg;
• Excipients: lactose monohydrate - 60.00 mg, croscarmellose sodium - 24.00 mg, colloidal silicon dioxide - 18.00 mg, microcrystalline cellulose - 165.00 mg, povidone (K = 30) - 21.00 mg, magnesium stearate - 12.00 mg;
• Film shell: Opadry OY-S-22898 yellow - 12.00 mg, consisting of: hypromellose - 6.5970 mg, titanium dioxide (E 171) - 3.9134 mg, sodium lauryl sulfate - 0.7096 mg, liquid paraffin - 0 .6760 mg, quinoline yellow dye (E 104) - 0.0750 mg, sunset yellow dye (E 110) - 0.0290 mg; liquid paraffin - 3.00 mg.

10 tablets in a blister pack (blister) [PVC/PVDC/aluminum foil].

3, 6 or 10 blisters along with instructions for use are placed in a cardboard box.

Description of the dosage form

Round, biconvex, film-coated tablets, pale yellow in color, scored on one side.

Cross-sectional appearance: uneven, granular surface, light yellow in color.

Characteristic

Thioctic acid is an endogenous antioxidant (binds free radicals); it is formed in the body during the oxidative decarboxylation of alpha-keto acids.

Directions for use and doses

Take 2 tablets (600 mg) of Berlition® 300 orally once a day. The daily dose is 600 mg.

The tablets are taken on an empty stomach, approximately 30 minutes before meals, without chewing, with a sufficient amount of liquid. Long-term use of the drug is possible.

The duration of the course of treatment and the possibility of its repetition is determined by the doctor.

Pharmacodynamics

Thioctic (alpha-lipoic) acid is an endogenous antioxidant of direct (binds free radicals) and indirect action. It is a coenzyme in the decarboxylation reactions of a-keto acids. Helps 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 breakdown products, reduces the formation of end products of progressive protein glycosylation in nerve cells in diabetes mellitus, improves microcirculation and endoneurial blood flow, and increases the physiological content of the antioxidant glutathione. By helping to reduce 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 swelling of the nervous tissue. Due to its participation in fat metabolism, thioctic acid increases the biosynthesis of phospholipids, in particular phosphoinoisitol, thereby improving the damaged structure of cell membranes; normalizes energy metabolism and the conduction of nerve impulses. Thioctic acid eliminates the toxic effects of alcohol metabolites (acetaldehyde, pyruvic acid), reduces the excessive formation of free oxygen radical molecules, reduces endoneurial hypoxia and ischemia, weakening the manifestations of polyneuropathy in the form of paresthesia, burning sensation, pain and numbness of the extremities.

Thus, thioctic acid has an antioxidant, neurotrophic, hypoglycemic effect, and improves lipid metabolism.

Use in the form of ethylenediamine salt reduces the severity of possible side effects of thioctic acid.

Pharmacokinetics

With intravenous administration of 600 mg of thioctic acid, the maximum concentration in blood plasma after 30 minutes is about 20 μg/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%).

Half-life up to 25 minutes. Total plasma clearance is 10-15 ml/min/kg.

Indications for use Berlition 300 mg 30 pcs. film-coated tablets

Diabetic polyneuropathy; alcoholic polyneuropathy.

Contraindications

History of hypersensitivity to thioctic (α-lipoic) acid, hypersensitivity to other components of the drug; pregnancy, breastfeeding period (there is no sufficient experience in using the drug); age under 18 years (the effectiveness and safety of the drug have not been established).

Application of Berlition 300 mg 30 pcs. film-coated tablets during pregnancy and breastfeeding

The use of Berlition® 300 during pregnancy is possible only if the expected benefit from therapy for the mother outweighs the potential risk to the fetus. Due to the lack of sufficient clinical experience with the use of Berlition® 300 during pregnancy and breastfeeding, its use in the corresponding categories of patients is not recommended.

special instructions

In patients with diabetes mellitus taking insulin or oral hypoglycemic drugs, constant monitoring of plasma glucose concentration is necessary, especially at the initial stage of therapy with Berlition®300. In some cases, it may be necessary to reduce the dose of insulin or oral hypoglycemic drugs to avoid the development of hypoglycemia.

When administered parenterally, hypersensitivity reactions may occur. If symptoms such as itching, nausea, malaise appear, treatment with Berlition® 300 should be stopped immediately.

Alcohol intake reduces the effectiveness of treatment with Berlition® 300, so patients during therapy with Berlition® 300 should refrain from drinking alcohol during the entire course of treatment, and also, if possible, in between courses.

The prepared solution of Berlition® 300 should be protected from exposure to light.

Impact on the ability to drive vehicles and operate machinery

The effect of Berlition® 300 on the ability to drive vehicles and operate machinery has not been specifically studied, therefore, during treatment with Berlition® 300, care should be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: nausea, vomiting, headache.

In severe cases: psychomotor agitation or clouding of consciousness, generalized convulsions, severe acid-base imbalance with lactic acidosis, hypoglycemia (up to the development of coma), acute necrosis of skeletal muscles, disseminated intravascular coagulation syndrome, hemolysis, suppression of bone marrow activity, multiple organ failure.

Treatment: If intoxication with thioctic acid is suspected (for example, taking more than 80 mg of the drug per 1 kg of body weight), emergency hospitalization and immediate application of measures in accordance with the general principles adopted for accidental poisoning are recommended. Therapy is symptomatic. Treatment of generalized seizures, lactic acidosis and other life-threatening consequences of intoxication should be carried out in accordance with the principles of modern intensive care. There is no specific antidote. Hemodialysis, hemoperfusion and filtration methods with forced removal of thioctic acid are not effective.

Side effects Berlition 300 mg 30 pcs. film-coated tablets

Possible side effects when using the drug Berlition®300 are listed below in descending frequency of occurrence: often (≥ 1/100,

From the nervous system - Very rarely: changes or disturbances in taste sensations, diplopia, convulsions.

From the hemostatic system - Very rare: purpura, thrombocytopathy.

Metabolic: Very rare: decreased plasma glucose levels (due to improved glucose absorption). Complaints indicative of a hypoglycemic state, such as dizziness, sweating, headache and blurred vision, have been reported.

On the part of the immune system - Very rarely: allergic reactions such as skin rash, urticaria (urticarial rash), itching, and in isolated cases - anaphylactic shock.

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

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

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.

Concomitant use of Berlition® 300 with cisplatin reduces the effectiveness of the latter.

Thioctic acid forms poorly soluble complex compounds with sugar molecules. Berlition® 300 is incompatible with solutions of glucose, dextrose, fructose, Ringer, as well as solutions that react with SH groups or disulfide bonds.

Berlition® 300 enhances the hypoglycemic effect of insulin and oral hypoglycemic drugs when used together.

Ethanol reduces the therapeutic effectiveness of Berlition® 300.

Directions for use and doses

IV, inside. For severe forms of polyneuropathy, 12-24 ml (300-600 mg alpha-lipoic acid) per day for 2-4 weeks. To do this, 1–2 ampoules of the drug are diluted in 250 ml of physiological 0.9% sodium chloride solution and administered dropwise over approximately 30 minutes. Subsequently, 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 alpha lipoic acid).