Berlition 300 mg 30 pcs. film-coated tablets

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.

Overdose of the drug Berlition

Overdose may cause nausea, vomiting and headache. When α-lipoic acid was used in very high doses (10–40 g), in combination with alcohol, severe intoxication, in some cases fatal, was observed. The clinical picture of intoxication at the beginning is manifested by psychomotor agitation or eclipse of consciousness, and later acquires a course with attacks of generalized convulsions and the development of lactic acidosis. Due to such intoxication, hypoglycemia, shock, rhabdomyolysis, hemolysis, disseminated intravascular coagulation, bone marrow suppression, and multiorgan failure may occur. Treatment of intoxication is carried out according to general principles: induce vomiting, wash the stomach, use sorbents. If necessary, carry out symptomatic therapy. Currently, there is no data on the advisability of hemodialysis, hemoperfusion or hemofiltration methods as part of the forced elimination of α-lipoic acid.

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.

Side effects of the drug Berlition

To assess the frequency of side effects, the following classification was taken as a basis: very often: ≤1/10; often: ≤1/100, but 1/10; sometimes: ≤1/1000, but 1/100; rare: ≤1/10,000, but 1/1000; very rare, including isolated cases: ≤1/10,000. Administration site reactions : reports have been very rare. Hypersensitivity reactions: allergic skin reactions in the form of urticaria, itching, eczema and skin rash, as well as systemic allergic reactions up to shock. Central nervous system disorders : very rarely - changes in taste sensations; convulsions, diplopia after intravenous administration. From the hematopoietic system: very rarely after intravenous administration - purpura and thrombocytopathy. General side effects: after rapid intravenous administration of the drug, there is a feeling of heaviness in the head and dyspnea, which goes away on its own. In some cases, blood sugar levels decrease due to an increase in the intensity of glucose absorption, which may be accompanied by symptoms similar to those of hypoglycemia - dizziness, sweating, headache and blurred vision.

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).

Interactions of the drug Berlition

α-lipoic acid forms complex compounds with metals (for example, with cisplatin), so its simultaneous use with cisplatin, iron and magnesium supplements, as well as with dairy products, due to their calcium content, is not recommended. Cisplatin should not be prescribed simultaneously with the use of Berlition due to a decrease in its effect under the influence of α-lipoic acid. α-Lipoic acid is capable of forming poorly soluble complex compounds with sugars contained in some infusion solutions, therefore the drug is incompatible with solutions of fructose, glucose, etc., as well as with solutions of drugs that are known to interfere reacting with SH groups or disulfide bridges.