Pharmacological properties
Pharmacodynamics. The active ingredient of the drug is thioctic acid, which acts as a coenzyme in the oxidative decarboxylation of α-keto acids; it plays an important role in the energy metabolism of the cell. In the amide form (lipoamide), it is an essential cofactor of multienzyme complexes that catalyze the decarboxylation of α-keto acids of the Krebs cycle. Thioctic acid has antitoxic and antioxidant properties, it is also able to restore other antioxidants, in particular in diabetes mellitus. In patients with diabetes mellitus, thioctic acid reduces insulin resistance and inhibits the development of peripheral neuropathy. It helps reduce blood glucose levels and glycogen accumulation in the liver. Thioctic acid affects the metabolism of carbohydrates, participates in the regulation of lipid and carbohydrate metabolism, and improves liver function (due to its hepatoprotective, antioxidant, and detoxification effects).
Pharmacokinetics. T ½ is 30 min. Total clearance is 694 ml/min. After a single administration, 93-97% of thioctic acid or its derivatives are excreted in the urine in the first 3-6 hours.
Indication
As part of the complex therapy of polyneuropathies of various genesis (diabetic and alcoholic polyneuropathy), liver diseases (hepatitis, cirrhosis).
Application
The drug is intended for intravenous injections/infusions after prior dilution in 0.9% sodium chloride solution.
For the prevention of diabetic polyneuropathy, in liver diseases, the dose of the drug is set individually, depending on the age, body weight of the patient and the severity of the disease. Treatment should be started with an initial dose of 10 ml (300 mg of thioctic acid) per day.
In severe diabetic polyneuropathy, treatment of adults begins with an infusion of 20 ml (600 mg) of thioctic acid diluted in 250 ml of 0.9% sodium chloride solution, 1 time per day for 1-2 weeks. Administer slowly - within 30 minutes (no more than 50 mg of thioctic acid in 1.7 ml of infusion solution per minute). In very severe liver diseases, the daily dose is increased to 900-1200 mg/day.
Contraindication
Hypersensitivity to the drug or to one of its components. Children's age. Pregnancy and breastfeeding.
Side effects
On the part of the gastrointestinal tract: in some cases, with rapid intravenous injection, nausea and vomiting are noted, which resolve on their own.
Neurological disorders: with rapid intravenous injection, a feeling of heaviness in the head, increased intracranial pressure, hot flashes, increased sweating, and difficulty breathing are possible.
In some cases, after administration, headache, dizziness, convulsions, diplopia, and visual disturbances are noted. In most cases, all of these symptoms disappear on their own.
From the side of the blood and lymphatic system: in some cases, after intravenous administration, petechial hemorrhages in the mucous membranes, skin, thrombocytopathies, platelet dysfunction, hypocoagulation, hemorrhagic rash (purpura), thrombophlebitis were observed.
Metabolic disorders: Hypoglycemia (dizziness, increased sweating, headache, visual impairment) is possible due to improved glucose utilization.
On the part of the immune system: when administered at the injection site, urticaria and the development of eczema, petechial rash, itching, dermatitis are possible. Rarely, systemic allergic reactions, up to anaphylactic shock.
Local reactions: in patients with hypersensitivity to Thioctodar, a burning sensation may occur at the injection site, which disappears on its own or when the rate of drug administration is reduced.
Cardiac disorders: pain in the heart area, tachycardia.
Special instructions
In the treatment of patients with diabetes mellitus, frequent monitoring of blood glucose is necessary. In some cases, dose adjustment of hypoglycemic agents is necessary to prevent hypoglycemia.
During the treatment of polyneuropathy, due to regenerative processes, a short-term increase in sensitivity is possible, which is accompanied by paresthesia with a feeling of "crawling ants."
Regular alcohol consumption is a risk factor for polyneuropathy and may reduce the effectiveness of Thioctodar. Therefore, it is recommended to refrain from drinking alcohol during treatment. Thioctodar should not be administered simultaneously with drugs containing metals (iron, magnesium, calcium preparations), as well as with dairy products containing calcium.
The drug is photosensitive, so the vials should be removed from the packaging only immediately before use.
Thioctodar solution prepared for infusion must be protected from sunlight by covering it with light-protective bags. Under these conditions, it remains suitable for no more than 6 hours.
Certain restrictions on the administration of thioctic acid preparations include old age (over 75 years old).
Use during pregnancy and breastfeeding. The drug Thioctodar is contraindicated during pregnancy. If necessary, its use during breastfeeding should be discontinued. Experimental studies have not revealed the teratogenic effect of thioctic acid. Similar studies have not been conducted in humans. There is no data on the excretion of thioctic acid into breast milk.
Children. Thioctodar is not recommended for use in children and adolescents due to the lack of clinical experience with the drug in this category of patients.
The ability to influence the reaction rate when driving vehicles or working with other mechanisms. No reports.
It is possible to increase the hypoglycemic effect when taking insulin or oral antidiabetic drugs. Thioctic acid reacts with ionic complexes of metals (for example, with cisplatin), so Thioctodar can reduce the effect of cisplatin. Thioctic acid forms poorly soluble complex compounds with glucose molecules. Thioctic acid is a metal chelator, so it is used simultaneously with metal preparations (for example, iron, magnesium preparations).
Incompatibility. Thioctodar is incompatible with glucose, fructose, Ringer's solution. The drug is incompatible with solutions containing compounds that react with SH groups or disulfide bridges.
Overdose
Nausea, vomiting, headache are possible. In case of overdose or suspected development of side effects, it is necessary to immediately stop the injection and, without removing the injection needle, slowly infuse 0.9% sodium chloride solution.
There is evidence that as a result of accidental or intentional use of thioctic acid in a dose of 10-40 g against the background of alcohol intoxication, isolated cases with serious signs of intoxication, including fatal outcome, were observed. Clinical symptoms of intoxication were manifested in the form of psychomotor agitation or dizziness with subsequent generalized convulsions and the development of lactic acidosis. The consequences of thioctic acid intoxication include hypoglycemia, shock, rhabdomyolysis, hemolysis, DIC, bone marrow suppression and multiple organ failure. In acute poisoning with thioctic acid, immediate hospitalization is indicated with general therapeutic measures for detoxification of the body (artificial respiration, artificially inducing vomiting, gastric lavage, use of activated charcoal, etc.). For the treatment of generalized convulsions, lactic acidosis and other consequences of intoxication, one should be guided by modern intensive care and a symptomatic approach to accelerate the elimination of thioctic acid. Further treatment is symptomatic.
Storage conditions
At a temperature not exceeding 25 °C in a place protected from light.
