Features of the drug
The main active ingredient in the medicine is thioctic acid in an amount of 300 or 600 ml. This vitamin-like substance belongs to the group of endogenous antioxidants. It is sometimes called vitamin N.
The active component in the drug binds free radicals, which in excess quantities can have a detrimental effect on the body. When using berlition, liver function improves. During therapy, lipid and carbohydrate metabolism is normalized. Thanks to its antioxidant activity, the drug protects cells from damage from the effects of decay products.
The medicine is produced in the form:
- A solution of a greenish tint, packaged in ampoules.
- Yellowish tablets placed in blisters.
The drug berlition, the instructions for use emphasize this, has different effects:
- Hypocholesterolemic. By lowering blood cholesterol levels, the risks of developing cardiovascular pathologies are reduced.
- Hepatoprotective. This allows you to protect the liver from the effects of toxic substances and accelerates the recovery of the organ in the treatment of various pathologies.
- Hypolipidemic. By normalizing lipid metabolism, it becomes possible to reduce the likelihood of developing obesity and atherosclerosis.
- Hypoglycemic. This reduces the risk of diabetes or developing a serious life-threatening condition against the background of the disease.
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.
Purpose of the drug
The drug berlition, the instructions for use confirm this, is used for various liver pathologies. Since the active substance in it normalizes metabolic processes, it is possible to increase the effectiveness of the main treatment.
The main indication for the use of berlition is alcoholic and diabetic polyneuropathy. This dangerous disease manifests itself with severe symptoms and gradual progression. It can only be slowed down with proper therapy.
Additionally, you can buy berlition for treatment:
- Fatty liver degeneration. This is a chronic disease that often occurs due to a sedentary lifestyle or heredity. In this case, healthy liver cells are replaced with lipids, which impairs the functioning of the organ.
- Steatohepatitis of various etiologies. Such diseases are characterized by the development of inflammatory processes that damage the organ.
- Intoxication of the body caused by various harmful substances.
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.
Treatment: recommended dosage
In the instructions for use, the manufacturer describes the standard treatment regimen with the drug. It can be changed in accordance with the recommendations of the attending physician. The individual course of treatment is based on the severity of the disease and the general condition of the patient.
Berlition tablets are intended for oral administration. As a rule, the medicine is prescribed once a day. Take it in the morning, half an hour before meals. In severe cases, the dosage is increased to two tablets per day.
The drug Berlition 600 is used for infusion administration. The initial daily dose is 600 mg. Since the active substance is photosensitivity, the solution is prepared immediately before use. To do this, one ampoule is diluted in 250 ml of 0.9% sodium chloride solution. The solution is injected slowly over at least 30 minutes. Aluminum foil is used for light protection.
It is allowed to carry out treatment with Berlition 600 for 2-4 weeks. If necessary, maintenance therapy with tablets is subsequently prescribed. The possibility of repeating the course is determined by the doctor individually based on an analysis of the patient’s condition.
Pharmacological properties of the drug Berlition
Pharmacodynamics. α-Lipoic acid (DL-5-(1,2-dithiolan-3-yl)-valeric acid) is a vitamin-like substance that is produced endogenously in the body. As a coenzyme, it participates in the oxidative decarboxylation of α-keto acids. In experimental diabetes mellitus, α-lipoic acid leads to a decrease in blood glucose levels and an increase in glycogen content in the liver, and in humans, to a change in the concentration of pyruvic acid in the blood serum. 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, resulting in decreased endoneural blood flow, endoneural ischemia, and increased production of free radicals that damage the peripheral nerve. The use of α-lipoic acid leads to a decrease in the formation of glycosylation products, improvement of endoneurial blood flow, and an increase in the content of the antioxidant glutathione, which leads to an improvement in the function of peripheral nerves in sensory diabetic polyneuropathy, namely: a decrease in the severity of pain, burning, sensation of numbness and “crawling” in the extremities . The use of α-lipoic acid also improves liver function when it is damaged. Pharmacokinetics. After oral administration, α-lipoic acid is rapidly absorbed into the gastrointestinal tract. Due to the significant effect of first pass through the liver, the absolute bioavailability of α-lipoic acid compared to IV administration is 20%. Due to rapid tissue distribution, the half-life in humans is 25 minutes, and the total plasma clearance is 10–15 ml/min/kg body weight. The maximum plasma level of 4 mcg/ml is achieved 30 minutes after oral administration of 600 mg of α-lipoic acid. At the end of a 30-minute infusion of 600 mg α-lipoic acid, its plasma level is approximately 20 mcg/ml. 80–90% of α-lipoic acid is excreted by the kidneys in the form of metabolites. Biotransformation occurs by oxidative reduction of the side chain and/or by S-methylation of the corresponding thiols.
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.
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.
Special instructions for the use of Berlition
During treatment with Berlition, alcohol consumption is strictly prohibited, since ethanol and its metabolites reduce the therapeutic effectiveness of the drug, as well as due to the risk of the onset and progression of polyneuropathy. Under the influence of α-lipoic acid, the hypoglycemic effect of insulin or oral antidiabetic agents may be enhanced, therefore, at the initial stage of treatment with Berlition, blood sugar levels should be monitored more frequently. In some cases, in order to prevent the onset of symptoms of hypoglycemia, it may be necessary to reduce the dose of insulin or the dose of an oral antidiabetic agent. Special security measures. With parenteral use of α-lipoic acid, hypersensitivity reactions have been observed, including the development of anaphylactic shock, so patients require appropriate medical supervision. If early symptoms appear, such as itching, nausea, or general malaise, you should immediately stop administering the drug. Use during pregnancy or breastfeeding. During pregnancy or breastfeeding, the drug is prescribed only according to strict indications and under the supervision of a doctor. There is no information regarding the penetration of α-lipoic acid into breast milk. Children. Children and adolescents under the age of 18 are excluded from the number of patients for whom Berlition is used due to the lack of sufficient experience with use. The ability to influence reaction speed when driving vehicles or other mechanisms : absent.
