Berlithion concentrate for solution for infusion 600ED (600mg)/24ml, 5 ampoules — Made in Germany — Free Delivery

Brand: Berlin-Chemie
Product Code: Berlithion
Availability: In Stock

$66.87

Description

Pharmacological properties

Pharmacodynamics. Thioctic acid is a vitamin-like substance formed in the body and performs the function of a coenzyme during the oxidative decarboxylation of α-keto acids. 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. this process leads to a decrease in endoneural blood flow and endoneural hypoxia / ischemia associated with an increased production of free oxygen radicals that damage the nerve, as well as depletion of an antioxidant such as glutathione in peripheral nerves.

In studies on rats, thioctic acid influenced the biochemical process caused by diabetes mellitus, which was triggered by streptozocin, decreased the formation of end products of progressive glycosylation, improved endoneural blood flow, increased the physiological content of glutathione, which acts in the nerve affected by the diabetic process similar to the action of an antioxidant relative to free oxygen radicals ... These effects suggest that thioctic acid may improve peripheral nerve function. This applies to sensory impairments that occur in polyneuropathy and can manifest as dysesthesias, paresthesias, such as pain, burning sensation, numbness or "creeping creeps." In 1995, a multicenter, placebo-controlled study was conducted to investigate the efficacy of thioctic acid for the symptomatic treatment of diabetic polyneuropathy, in which data were obtained on the beneficial effects of thioctic acid on such studied symptoms as paresthesias, burning sensation, numbness and pain.

Pharmacokinetics. Thioctic acid is highly susceptible to the effect of the primary passage through the liver. Systemic bioavailability is characterized by significant individual variations. Biotransformation of thioctic acid occurs by side chain oxidation and conjugation and is excreted mainly by the kidneys. T½ of thioctic acid in humans is about 25 minutes, and the total clearance in blood plasma is 10-15 ml / min / kg. After a 30-minute infusion of 600 mg of thioctic acid, its plasma concentration is about 20 μg / ml. In experiments on animals (rats, dogs), using a radioactive label, it was possible to reveal the predominant excretion by the kidneys (80-90%), namely, in the form of metabolites. In humans, there is also only a small amount of excreted intact substance in the urine. Metabolism occurs mainly by side chain oxidation (β-oxidation) and / or by S-methylation of the corresponding thiols.

Thioctic acid interacts in vitro with ionic metal complexes (for example, with cisplatin).

Thioctic acid forms poorly soluble complex compounds with sugar molecules.

Indications

Paresthesia in diabetic polyneuropathy.

Application

Adults

Doses. In case of intense paresthesias caused by diabetic polyneuropathy, it is recommended to intravenously administer a concentrate for an infusion solution at a dose of 12 ml (1 ampoule of Berlithion 300 U) to 24 ml (2 ampoules of Berlithion 300 U or 1 ampoule of Berlithion 600 U) per day , which corresponds to 300-600 mg of thioctic acid per day.

Mode of application. After dilution, the concentrate for the preparation of the solution for infusion is used intravenously for 2-4 weeks at the initial stage of treatment. The contents of 1 or 2 ampoules of the preparation Berlithion 300 U or 1 ampoule of Berlithion 600 U are diluted in 250 ml of 0.9% sodium chloride solution and administered intravenously, the duration of the infusion should be at least 30 minutes. Due to the sensitivity of the active substance to light, an infusion solution is prepared immediately before administration and protected from light, for example, using aluminum foil. The prepared solution for infusion can be stored for 6 hours, provided it is protected from light.

For further therapy, oral forms of thioctic acid are indicated at a dose of 300–600 mg / day.

Pediatric population. No data available.

The basis for the treatment of diabetic polyneuropathy is the optimal correction of the patient's blood glucose level.

Contraindications

History of hypersensitivity to thioctic acid or other components of the preparation.

Side effects

Classification of the frequency of adverse reactions: very often (≥1 / 10); often (from? 1/100 to 1/10); infrequently (from ≥1 / 1000 to 1/100); rarely (from ≥1 / 10,000 to 1/1000); very rare (1/10 000); unknown (frequency cannot be determined from available data).

On the part of the hematopoietic system: in some cases, petechial hemorrhages in the mucous membranes / skin, hypocoagulation, thrombophlebitis were observed; very rarely - after intravenous administration of thioctic acid, hemorrhagic rash (purpura), dysfunction of platelets were observed.

From the immune system: unknown - autoimmune insulin syndrome (see SPECIAL INSTRUCTIONS). Skin allergic reactions may occur in the form of rash, hives, itching, eczema, as well as systemic reactions up to the development of shock.

From the side of the central nervous system: very rarely - changes or disturbances in taste, headache, hot flashes, increased sweating, dizziness, visual impairment. After intravenous administration of thioctic acid, convulsions were observed, as well as double vision. In most cases, all these manifestations go away on their own; unknown - loss of consciousness, seizures.

On the part of the digestive tract: in some cases, with rapid intravenous administration of the preparation, nausea, vomiting, diarrhea, and abdominal pain were observed, which passed on their own.

From the hepatobiliary system: unknown - cholestatic hepatitis.

Metabolic disorders: very rarely - due to improved absorption of glucose, its level in the blood may decrease, as a result of which symptoms similar to those of hypoglycemia, such as dizziness, increased sweating, headache, visual impairment, may appear.

From the side of the cardiovascular system: with a rapid intravenous injection, pain in the region of the heart, tachycardia, which pass on their own, are possible.

General disorders and reactions at the injection site: often - after a quick intracranial injection, an increase in intracranial pressure, shortness of breath, which pass on their own, are possible; very rarely - in isolated cases, a reaction at the injection site and weakness were reported.

Possible adverse reactions reported. Reports on possible adverse reactions after registration of a medicinal product play an important role. This allows you to continue monitoring the benefit / risk ratio when using this preparation. Health workers are required to report any potential adverse reactions through the national reporting system.

Special instructions

With parenteral use of thioctic acid, hypersensitivity reactions were observed up to the development of anaphylactic shock. therefore, appropriate supervision of patients is necessary. if early symptoms appear (for example, itching, nausea, weakness, etc.), treatment should be stopped immediately; under certain circumstances, it is necessary to carry out further therapeutic measures.

Cases of the development of autoimmune insulin syndrome (AIS) during treatment with thioctic acid have been reported. Patients with the human leukocyte antigen genotype (alleles HLA-DRB1 * 04: 06 and HLA-DRB1 * 04: 03) are more likely to develop AIS when treated with thioctic acid. Alleles HLA-DRB1 * 04: 03 (coefficient of susceptibility of AIS development - 1.6) are especially common among representatives of the Caucasian race (more in Southern Europe than in Northern Europe), and alleles HLA-DRB1 * 04: 06 (coefficient of susceptibility of AIS development - 56.6) are especially common in patients of Japanese and Korean nationality.

AIS should be considered in the differential diagnosis of spontaneous hypoglycemia in patients receiving thioctic acid treatment.

The main factor in effective treatment for diabetic polyneuropathy is the optimal correction of blood glucose levels. When treating patients with diabetes mellitus, especially at the beginning of therapy, frequent monitoring of blood glucose is required. In some cases, a dose adjustment of antidiabetic agents is required to prevent hypoglycemia. During the treatment of polyneuropathy, due to regeneration processes, a short-term increase in sensitivity is possible, which is accompanied by paresthesia with a feeling of "creeping".

Drinking alcohol can reduce the effectiveness of the preparation, therefore it is recommended to refrain from drinking alcohol during preparation treatment.

The preparation is photosensitive, therefore, the vials should be taken out of the package only immediately before use.

A certain limitation for intravenous administration of thioctic acid preparations is the elderly age of the patient (75 years).

Use during pregnancy and lactation. In accordance with the general principles of pharmacotherapy, preparations during pregnancy and breastfeeding can be used only after a careful assessment of the benefit / risk ratio.

Pregnant and breastfeeding women should be treated with thioctic acid only strictly according to the indications determined by the doctor, although reproductive toxicity studies have not revealed any effect on fertility and early development of the embryo. No embryotoxic properties have been identified in studies either.

There are no data on the penetration of thioctic acid into breast milk.

Children. The preparation Berlithion is not intended for the treatment of children and adolescents due to the lack of clinical experience.

The ability to influence the reaction rate when driving or operating machinery. During the use of the preparation, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions, since adverse reactions from the nervous system and the organ of vision are possible.

Interactions

Thioctic acid interacts in vitro with ionic metal complexes (for example, with cisplatin), therefore there were reports of a decrease in the effectiveness of cisplatin while being treated with the preparationBerlithion 300 units or Berlithion 600 units.

With sugar molecules (for example, with a solution of fructose) thioctic acid forms difficult-to-dissolve complex compounds.

Thioctic acid is a metal chelator, so it cannot be used together with metals (iron and magnesium preparations).

Thioctic acid can enhance the hypoglycemic effect of insulin and / or other antidiabetic agents, therefore, especially at the beginning of treatment with thioctic acid, regular monitoring of blood glucose levels is indicated. To prevent the onset of symptoms of hypoglycemia, in some cases, it may be necessary to reduce the dose of insulin and / or oral antidiabetic agents.

Note. Regular alcohol consumption is a significant risk factor for the onset and progression of the clinical picture of neuropathy and, thus, may interfere with the effectiveness of treatment with Berlithion 300 IU or Berlithion 600 IU. Therefore, patients with diabetic polyneuropathy are strongly advised to stop drinking alcohol. This also applies to periods when therapy is not carried out.

Incompatibility. Thioctic acid interacts in vitro with ionic metal complexes (for example, with cisplatin). Thioctic acid forms poorly soluble complex compounds with sugar molecules (for example, with a solution of fructose).

Berlithion 300 U or Berlithion 600 U is incompatible with glucose solutions, Ringer's solution, as well as with solutions reacting with SH-groups or disulfide bridges.

For the use of the preparation Berlithion 300 IU or Berlithion 600 IU in the form of infusion, only physiological solution of sodium chloride is used as a carrier solution.

Overdose

Overdose may cause nausea, vomiting, and headache. if taken accidentally or used in very high doses - 10-40 g of thioctic acid in combination with alcohol, severe intoxication is noted, which can lead to death. the clinical picture of poisoning is initially manifested by psychomotor agitation or impaired consciousness, and in the future its course is accompanied by attacks of generalized seizures and the development of lactic acidosis. in addition, the consequences of intoxication with high doses of thioctic acid can be hypoglycemia, shock, rhabdomyolysis, hemolysis, blood ICE, bone marrow suppression and multiple organ failure.

Treatment. If significant intoxication is suspected (for example, 80 mg / kg body weight of thioctic acid in adults and 50 mg / kg body weight of thioctic acid in children), immediate hospitalization and standard measures are indicated in accordance with the principles of treatment of poisoning (for example, induction of vomiting, gastric lavage, reception of activated carbon, etc.). Treatment of attacks of generalized seizures, lactic acidosis and other consequences of intoxication that threaten the patient's life should be based on modern principles of intensive care and be symptomatic. At the moment, there are no data on the advisability of using hemodialysis, hemoperfusion methods or hemofiltration in the framework of the forced excretion of thioctic acid.

Storage conditions

Store ampoules in a cardboard box to protect them from light.

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