Instructions for Lipothion injection solution 600 mg/50 ml bottle 50 ml No. 1
Composition
active ingredient: thioctic (α-lipoic) acid;
1 bottle (50 ml) of solution contains thioctic (α-lipoic) acid 600 mg;
excipients: trometamol, sodium chloride, 1M trometamol solution, water for injection.
Dosage form
Solution for injection.
Main physicochemical properties: transparent solution of light yellow color.
Pharmacotherapeutic group
Drugs affecting the digestive system and metabolic processes. Thioctic acid. ATC code A16A X01.
Pharmacological properties
Pharmacodynamics.
α-Lipoic acid is a vitamin-like substance of endogenous origin that functions as a coenzyme in the oxidative decarboxylation of α-keto acids.
Hyperglycemia caused by diabetes leads to the accumulation of so-called “advanced glycation end products.” This process leads to reduced endoneural blood flow and endoneural hypoxia and ischemia, accompanied by increased production of oxygen free radicals, which in turn damage the peripheral nerve. There is also a decrease in the level of antioxidants such as glutathione in the peripheral nerves.
α-Lipoic acid intervened in these processes, leading to a decrease in the formation of glycation end products, improved endoneural blood flow, and increased physiological levels of antioxidants such as glutathione, which is an antioxidant for free oxygen radicals in the diabetic nerve.
These effects observed in the experiment support the theory that peripheral nerve function can be improved by α-lipoic acid. This applies to sensory disturbances in diabetic polyneuropathy, manifested by dysesthesia, paresthesias such as burning sensations, pain, numbness, and "creeping sensations."
Pharmacokinetics.
The primary transformation of α-lipoic acid occurs in the liver. There is no significant difference in the systemic availability of α-lipoic acid between patients. α-lipoic acid is biotransformed by side-chain oxidation and conjugation and is excreted mainly by the kidneys.
The plasma half-life of α-lipoic acid in humans is approximately 25 minutes, and the total plasma clearance is 10–15 ml/min per kilogram. At the end of a 12-minute infusion of 600 mg, the plasma concentration is approximately 47 μg/ml. In animal studies (rats, dogs), radiolabeling has shown that renal excretion is predominantly in the form of metabolites, accounting for 80–90%. In humans, only a small fraction of the intact substance is found in the urine. Biotransformation occurs mainly by oxidation of the side chains (beta-oxidation) and/or S-methylation of the corresponding thiol groups.
Indication
Treatment of symptoms of peripheral (sensorimotor) diabetic polyneuropathy.
Contraindication
Hypersensitivity to the active substance and/or to the excipients of the medicinal product.
Interaction with other medicinal products and other types of interactions
When used simultaneously with thioctic acid, the effectiveness of cisplatin is reduced.
When used simultaneously with thioctic acid, the blood sugar-lowering effect of insulin and/or other antidiabetic agents may be enhanced. In the case of simultaneous use of such drugs, especially at the beginning of treatment, regular monitoring of blood glucose levels should be carried out. To prevent the appearance of symptoms of hypoglycemia, in individual cases it may be necessary to reduce the dose of insulin and/or oral antidiabetic agents.
WARNING.
Regular alcohol consumption is a significant risk factor for the development and progression of the clinical picture of neuropathy and can thus negatively affect the course of treatment with thioctic acid. Therefore, patients with diabetic polyneuropathy are usually advised to abstain from alcohol consumption if possible. This restriction also applies to breaks between courses of treatment.
Application features
With parenteral administration of thioctic acid, hypersensitivity reactions of varying severity up to anaphylactic shock have been observed (see section "Adverse reactions"). During the administration of the drug, patients should be under close medical supervision. If the first signs appear (itching, nausea, weakness), treatment should be stopped immediately and, if necessary, appropriate assistance should be provided.
After the use of thioctic acid, an unusual odor of urine may be observed; this phenomenon is not clinically significant.
The drug contains 52.487 mg/vial of sodium, so caution should be exercised when administering it to patients on a controlled sodium diet.
Use during pregnancy or breastfeeding
The drug is not recommended for use during pregnancy due to the lack of relevant clinical data.
There is no data on the penetration of thioctic acid into breast milk, therefore the drug is not recommended for use during breastfeeding.
Ability to influence reaction speed when driving vehicles or other mechanisms
Thioctic acid has no or negligible effect on the reaction rate when driving or using other mechanisms.
Method of administration and doses
The drug is intended for intravenous administration.
The basis of treatment for diabetic polyneuropathy is optimal diabetic control.
Dosage.
Doses and duration of treatment are set individually.
In the presence of symptoms of peripheral (sensorimotor) diabetic polyneuropathy, the recommended daily dose for adults is 50 ml of injection solution (corresponding to 600 mg of thioctic acid per day) intravenously.
During the initial treatment period, the injection solution should be administered intravenously for 2–4 weeks.
Method of application.
The solution should be administered intravenously drip over 30 minutes, after diluting the ampoule of the drug in 250 ml of 0.9% sodium chloride solution. Only 0.9% sodium chloride solution should be used to prepare the infusion solution.
Intravenous administration can be done without dilution using an injection syringe over a period of at least 12 minutes.
Infusion rules.
Since the active substance of the medicinal product is sensitive to light, the solution for short-term infusion should be prepared immediately before use.
The infusion solution should be protected from light (e.g. by using aluminium foil). The infusion solution protected from light is suitable for approximately 6 hours. Care should be taken to ensure that the infusion time is at least 12 minutes.
It is recommended to continue treatment with thioctic acid in oral forms at a dose of 600 mg per day.
Children.
The medicine should not be used in children.
Overdose
Symptoms.
In case of overdose, nausea, vomiting, and headache may occur.
As a result of accidental or intentional use of thioctic acid in a dose of 10-40 g during alcohol intoxication, isolated cases with severe signs of intoxication, including fatal outcome, were observed. Clinical manifestations of intoxication were manifested in the form of psychomotor impairment or dizziness with subsequent generalized convulsions and the development of lactic acidosis. The consequences of thioctic acid intoxication are hypoglycemia, shock, rhabdomyolysis, hemolysis, disseminated intravascular coagulation (DIC), bone marrow suppression and multiple organ failure.
Treatment.
If significant intoxication with thioctic acid is suspected (for example, more than 10 tablets of 600 mg for adults and more than 50 mg/kg of body weight for children), the patient should be immediately hospitalized and standard measures for the treatment of intoxication should be initiated (induction of vomiting, gastric lavage, administration of activated charcoal). Treatment of generalized convulsions, lactic acidosis and other life-threatening consequences of intoxication should be based on the principles of modern intensive care and be aimed at eliminating symptoms.
To date, no advantages of hemodialysis, hemoperfusion, or filtration methods in the forced removal of thioctic acid have been identified.
Side effects
Adverse reactions that may occur during the use of thioctic acid are classified according to the following frequency: very common (≥1/10), common (≥1/100 - <1/10), uncommon (≥1/1000 - <1/100), rare (≥1/10000 - <1/1000), very rare (<1/10000), frequency unknown (cannot be estimated from the available data).
Blood and lymphatic system disorders:
very rarely - thrombopathy.
On the part of the immune system:
frequency unknown - allergic reactions such as skin rashes, urticaria, eczema, itching; anaphylactic reactions, autoimmune insulin syndrome (see section "Special warnings and precautions for use").
Metabolism and nutrition:
very rarely - hypoglycemia*.
From the nervous system:
uncommon – dysgeusia; very rare – apoplexy, headache*, dizziness*, increased sweating*.
On the part of the organs of vision:
very rarely - diplopia, visual disturbances.
From the digestive tract:
infrequently - nausea and vomiting.
Skin and subcutaneous tissue disorders:
very rarely - purpura.
On the part of the body as a whole and reactions at the injection site:
very rarely - reactions at the injection site.
After rapid intravenous injection, a feeling of pressure in the head and difficulty breathing may occur, which resolve on their own.
*Due to the improved glucose excretion, in very rare cases a decrease in blood glucose levels may occur. Symptoms of hypoglycemia such as dizziness, increased sweating, headache and blurred vision have been reported in this regard.
Reporting suspected adverse reactions that occur after the registration of a medicinal product is very important. This allows for continuous monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals should report any suspected adverse reactions through the national pharmacovigilance system.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C in a place protected from light and out of the reach of children.
Incompatibility.
Thioctic acid reacts in vitro with metal ion complexes (e.g., cisplatin). Thioctic acid forms complex compounds with sugar molecules (e.g., levulose solution).
The drug is incompatible with glucose solution, Ringer's solution, as well as with solutions known to react with SH groups or disulfide bonds.
Only 0.9% sodium chloride solution should be used as a carrier solution for infusions of the medicinal product.
Packaging
50 ml in a bottle; 1 bottle in a light-protective case; 1 light-protective case in a cardboard box.
Vacation category
According to the recipe.
Producer
Mefar Ilach San. A.Sh./Mefar Ilac San. AS
Location of the manufacturer and address of its place of business.
Ramazanoglu Mach. Ansar Jad. No. 20, 34906 Kurtkoy – Pendik/Istanbul, Turkey/Ramazanoglu Mah. Ensar Cad. No: 20, 34906 Kurtkoy – Pendik/Istanbul, Turkey.
Applicant.
WORLD MEDICINE LLC, Ukraine/WORLD MEDICINE, LLC, Ukraine.
