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.
Berlition 300 (conc. solution 25 mg/ml 12 ml No. 5)
A country
Germany
The country of production may vary depending on the batch of goods. Please check with the operator for detailed information when confirming your order.
Active substance
Thioctic acid
Compound
Active ingredient (per 1 ampoule of 12 ml): thioctic acid - 0.300 g. Excipients: ethylenediamine, propylene glycol, water for injection. Description: Transparent greenish-yellow solution. Release form Concentrate for the preparation of solution for infusion, 25 mg/ml. 12 ml of the drug in dark glass ampoules with a white ring (break line) in the upper part of the ampoule. 5 ampoules per cardboard contour package (tray). 1, 2 or 4 cardboard contour packages with instructions for use of the drug in a cardboard box.
Pharmacological properties
Pharmacodynamics Thioctic (alpha-lipoic) acid is an endogenous antioxidant of direct (binds free radicals) and indirect action. This is a vitamin-like substance, a coenzyme for the decarboxylation reactions of α-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 nerve 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 content of the antioxidant glutathione to physiological levels. 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 endoneural 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. Pharmacokinetics Distribution With intravenous administration of 600 mg of thioctic acid, the maximum concentration in blood plasma after 30 minutes is about 20 mcg/ml, the area under the concentration-time curve is about 5 mcg/h/ml. Bioavailability - 30%. Metabolism and excretion Has a “first pass” effect through the liver. Thioctic acid undergoes biotransformation primarily through oxidative shortening of the side chain (beta-oxidation) and/or through S-methylation of the corresponding thiols. Volume of distribution is about 450 ml/kg. Total plasma clearance is 10-15 ml/min/kg. Excreted by the kidneys (80-90%) mainly in the form of metabolites. The half-life is about 25 minutes.
Indications for use
diabetic polyneuropathy; alcoholic polyneuropathy.
Contraindications
history of hypersensitivity to thioctic acid or 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). Caution: Intravenous administration of thioctic acid should be used with caution in elderly patients (over 75 years of age). Use during pregnancy and breastfeeding Due to the lack of sufficient clinical experience with the use of thioctic acid during pregnancy and breastfeeding, the use of the drug is contraindicated.
Mode of application
For intravenous administration. At the beginning of treatment, Berlition ® 300 is prescribed intravenously in a daily dose of 600 mg (2 ampoules). Before use, the contents of 2 ampoules (24 ml of the drug) are diluted in 250 ml of 0.9% sodium chloride solution and administered intravenously slowly over at least 30 minutes. Since the active substance is sensitive to light, the solution for infusion is prepared immediately before use. The prepared solution must be protected from light, for example, using aluminum foil. The solution, protected from light, can be stored for about 6 hours. The course of treatment with Berlition ® 300 is 2-4 weeks. Then they switch to maintenance oral therapy at a dose of 600 mg per day. The duration of the course of treatment and the need to repeat it is determined by the doctor. Therapy for diabetic polyneuropathy should be aimed at correcting the underlying disease—diabetes mellitus.
Side effect
Possible side effects when using the drug Berlition ® 300 are listed below in descending frequency of occurrence: often (≥ 1/100, disorders of the hematopoietic and lymphatic system very rarely: petechial hemorrhages in the mucous membranes, skin; hemorrhagic rash (purpura), thrombocytopathy, hypocoagulation Immune system disorders Very rare: allergic reactions (skin rash, eczema, urticaria, itching) Frequency unknown: anaphylactic shock, autoimmune insulin syndrome in patients with diabetes mellitus, which is characterized by frequent hypoglycemia in the presence of autoantibodies to insulin. Metabolic and nutritional disorders Very rare: hypoglycemia (due to improved absorption of glucose), symptoms of which include dizziness, increased sweating, headache and blurred vision Nervous system disorders Very rare: change or disturbance in taste sensations, hot flashes ", convulsions. Gastrointestinal disorders. Common: nausea, vomiting; Very rare: abdominal pain, diarrhea. Disorders of the liver and biliary tract Very rarely: increased activity of liver enzymes. Cardiac disorders Frequency unknown: pain in the heart area, tachycardia with rapid administration of the drug. Vascular disorders Very rare: thrombophlebitis. Visual disturbances: Very rare: diplopia, blurred vision. General disorders and disorders at the injection site Very rare: burning sensation at the injection site; Frequency unknown: allergic reactions at the injection site - irritation, redness or swelling. Other Very rare: with rapid intravenous administration, a spontaneous increase in intracranial pressure (a feeling of heaviness in the head) and difficulty breathing, weakness were observed.
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 (DIC syndrome), hemolysis, suppression of bone function. brain, multiple organ failure. Treatment: If intoxication with thioctic acid is suspected (for example, the use of more than 80 mg of thioctic acid per 1 kg of body weight in adults and more than 50 mg of thioctic acid per 1 kg of body weight in children), emergency hospitalization and immediate application of measures in accordance with general principles adopted in case of accidental poisoning. 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 ineffective.
Interaction
Due to the fact that thioctic acid is capable of forming chelate complexes with metals (including cisplatin), simultaneous use with iron, magnesium and calcium preparations should be avoided. The simultaneous use of thioctic acid with cisplatin reduces the effectiveness of the latter. Thioctic acid forms poorly soluble complex compounds with sugar molecules. Thioctic acid is incompatible with solutions of glucose, dextrose, fructose, Ringer, as well as with solutions that react with SH groups or disulfide bonds. Thioctic acid enhances the hypoglycemic effect of insulin and hypoglycemic drugs for oral administration when used simultaneously. Ethanol significantly reduces the therapeutic effectiveness of thioctic acid.
special instructions
In patients with diabetes mellitus receiving insulin or oral hypoglycemic drugs, constant monitoring of plasma glucose concentrations 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 during avoiding the development of hypoglycemia. When administered parenterally, hypersensitivity reactions may occur, including the development of anaphylactic shock. 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, therefore patients during therapy with Berlition ® 300 should refrain from drinking alcohol during the entire course of treatment, and also, if possible, during the break between courses. There have been reports of cases of the development of autoimmune insulin syndrome (AIS) during treatment with thioctic acid. Patients with the HLA-DRB*04:06 and HLA-DRB1*04:03 alleles in their leukocyte antigen genotype are more susceptible to developing AIS during treatment with thioctic acid. The HLA-DRB1*04:03 allele (odds ratio for developing AIS is 1.6) is predominantly found in Caucasians (with a higher prevalence in Southern Europe than in Northern Europe), and the HLA-DRB*04:06 allele (odds ratio for developing AIS - 56.6) is primarily found among Japanese and Korean patients. Autoimmune insulin syndrome should be taken into account in the differential diagnosis of spontaneous hypoglycemia in patients taking thioctic acid. The solvent for Berlition ® 300 can only be a 0.9% sodium chloride solution. A freshly prepared solution of Berlition ® 300 for infusion should be protected from light, for example, with aluminum foil and stored for 6 hours. The effect of the drug on the ability to drive vehicles and machinery. The effect of thioctic acid on the ability to drive vehicles and operate machinery has not been specifically studied, therefore, during treatment with Berlition ® 300, caution should be exercised when driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Dispensing conditions in pharmacies
On prescription
Use of the drug Berlition
Diabetic and alcoholic polyneuropathy. The drug Berlition 300 capsules, Berlition 300 oral - in the form of film-coated tablets, taken orally 2 capsules 1 time per day; drug Berlition 600 capsules - 1 capsule 1 time per day 30 minutes before the first meal. In case of severe disease, during the first 1–2 weeks of treatment, combined administration of the drug (IV and orally) is used: in the morning, IV administration of 24 ml/day of the drug Berlition 600 IU in the form of a concentrate for preparing a solution for infusion or 12– 24 ml of a solution of the drug Berlition 300 IU in the form of a concentrate for preparing a solution for infusion , and in the evening - take the drug in the form of capsules or tablets of Berlition 300 or 600 mg. To dilute the drug Berlition 300 or 600 units, only 0.9% sodium chloride solution is used. The contents of the ampoule are diluted with 250 ml of this solution and administered intravenously for at least 30 minutes. The solution of the drug must be protected from exposure to sunlight (for example, wrap the bottle with aluminum foil). If this condition is met, the diluted solution can be stored for 6 hours. For further treatment, 300–600 mg of α-lipoic acid is used in the form of Berlition 300 or 600 mg tablets or capsules. The course of treatment is at least 2 months; if necessary, it can be carried out 2 times a year. Berlition 300 units be administered intramuscularly by injection in a dose not exceeding 2 ml; IM injection sites should be constantly changed. The course of treatment is 2–4 weeks. of Berlition 300 oral, 1–2 tablets per day for 1–2 months, is indicated as maintenance therapy Liver diseases. The drug is prescribed in accordance with the above scheme at a dose of 600–1200 mg of α-lipoic acid per day, depending on the severity of the condition and laboratory indicators of the functional state of the patient’s liver.
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.
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.
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.
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.
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.
