Instructions Espa-Lipon injection 600 solution for injection 600 mg ampoule 24 ml No. 5
Composition
active ingredient: thioctic acid; 1 ampoule of the drug injection 600 (24 ml) contains 755 mg of thioctic acid ethylenediamine salt (equivalent to 600 mg of thioctic acid)
excipient: water for injections.
Dosage form
Solution for injection.
Main physicochemical properties: transparent solution of greenish-yellow color.
Pharmacotherapeutic group
Drugs that affect the digestive system and metabolic processes. Thioctic acid.
ATX code A16A X01.
Pharmacological properties
Pharmacodynamics
Thioctic acid is a substance that is formed in the body and acts as a coenzyme in the oxidative decarboxylation of a-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 increased formation of free oxygen radicals that damage the nerve, as well as to the depletion of such an antioxidant as glutathione in peripheral nerves. In 1995, a multicenter placebo-controlled study was conducted to study the effectiveness of using thioctic acid for the symptomatic treatment of diabetic polyneuropathy, which obtained data on the beneficial effects of thioctic acid on such studied symptoms as paresthesia, burning sensation, numbness and pain.
Pharmacokinetics
Thioctic acid has a high first-pass effect in the liver. There are significant interindividual differences in the systemic availability of thioctic acid. Biotransformation of thioctic acid occurs by oxidation of side chains and fusion. Excretion is mainly renal.
In humans, the plasma half-life is about 25 minutes, the total plasma clearance is 10-15 ml/min.kg. At the end of a 30-minute infusion of 600 mg, the determined plasma level is about 20 μg/ml. Radiolabeling in animal studies (rats, dogs) revealed that 80-90% of the drug is excreted predominantly as metabolites. In humans, only a small amount of unchanged substance is excreted in the urine. Biotransformation occurs mainly by oxidative reduction of side chains (beta-oxidation) and/or S-methylation of thiol groups.
Indication
Treatment of diabetic polyneuropathy.
Contraindication
Hypersensitivity to thioctic acid or to one of the other components of the drug.
Interaction with other medicinal products and other types of interactions
Thioctic acid reacts with metal ion complexes (for example, with cisplatin), so the drug may reduce the effect of cisplatin.
With sugar molecules (for example, with a solution of levulose), thioctic acid forms poorly soluble complex compounds.
Thioctic acid is a metal chelator, so it cannot be used together with metals (for example, iron, magnesium preparations).
Thioctic acid may enhance the hypoglycemic effect of insulin and oral antidiabetic agents, increasing the sensitivity of peripheral tissues to these drugs, which may require adjustment of the dose of insulin or oral antidiabetic agents. For this reason, careful monitoring of blood sugar is necessary, especially at the initial stage of therapy.
Note
Regular alcohol consumption is a significant risk factor for the development and progression of neuropathic syndromes and may therefore affect the success of treatment with Espa-lipon®. Therefore, patients with diabetic polyneuropathy are generally advised to avoid alcohol consumption. This also applies to intervals when therapy is not being administered.
Application features
The main principle of treatment of diabetic polyneuropathy is optimal control of diabetes. Frequent monitoring of glycemia is necessary in the treatment of patients with diabetes. In some cases, it is necessary to adjust the doses of hypoglycemic agents to prevent hypoglycemia.
During the treatment of polyneuropathy, due to regeneration processes, a short-term increase in sensitivity is possible, accompanied by paresthesia with a feeling of "crawling ants."
Regular alcohol consumption is a risk factor for polyneuropathy and may reduce the effectiveness of the drug. Therefore, it is recommended to refrain from drinking alcohol during treatment with the drug. The drug should not be prescribed simultaneously with drugs containing metals (iron, magnesium, calcium drugs), as well as with dairy products containing calcium.
The drug is light-sensitive, so the vials should be removed from the packaging only immediately before use.
The prepared solution for infusion must be protected from sunlight by covering it with light-protective bags. Under these conditions, it remains suitable for a maximum of 6 hours.
Hypersensitivity reactions, including anaphylactic shock, have been observed with parenteral use of Espa-lipon® (see section "Adverse reactions"). Appropriate monitoring of patients is necessary. In the event of early symptoms (e.g. itching, nausea, discomfort, etc.), therapy should be discontinued immediately; additional therapeutic measures may be necessary.
Ability to influence reaction speed when driving vehicles or other mechanisms
During treatment, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Use during pregnancy or breastfeeding
The use of thioctic acid during pregnancy is not recommended due to the lack of relevant clinical data.
There is no data on the penetration of thioctic acid into breast milk, therefore its use during breastfeeding is not recommended.
Method of administration and doses
Adults are given 12-24 ml of solution in 250 ml of 0.9% sodium chloride solution once a day (equivalent to 300 mg or 600 mg of thioctic acid per day).
The solution is administered as an intravenous infusion; it is used for 2-4 weeks at the initial stage of treatment.
As a further continuation of therapy, Espa-lipon® 600 (in tablet form) can be used.
Infusion rules
For the preparation of the infusion solution, only 0.9% sodium chloride solution should be used. The drug should be administered intravenously drip for at least 30 minutes, before which the Espa-lipon® ampoule is diluted in 250 ml of 0.9% sodium chloride solution. The drug is sensitive to sunlight, so the solution should be prepared immediately before the start of the administration and the prepared bottle should be protected with a light-protective cap. The infusion solution protected from light can be stored for about 6 hours.
Children
Since there are no data on the safety and efficacy of thioctic acid in children, the drug is not recommended for use in this age group of patients.
Overdose
Overdose may cause nausea, vomiting, headache. In case of overdose or suspected side effects, the injection should be stopped immediately and, without removing the injection needle, a slow infusion of 0.9% sodium chloride solution should be carried out through it.
Treatment. In acute poisoning with thioctic acid, immediate hospitalization is indicated with general therapeutic measures for detoxification of the body (artificial respiration, vomiting, gastric lavage, 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 excretion of thioctic acid. Therapy is symptomatic.
Adverse reactions
On the part of the digestive tract: in some cases, nausea and vomiting are observed with rapid intravenous injection, which resolve on their own.
From the nervous system: change or disturbance of taste sensations; with rapid intravenous injection, a feeling of heaviness in the head, increased intracranial pressure, hot flashes, increased sweating, difficulty breathing are possible. In some cases, headache, dizziness, convulsions, diplopia, visual impairment were observed after intravenous administration. In most cases, all these manifestations resolve on their own.
On the part of the blood system: in some cases, after intravenous administration, petechial hemorrhages in the mucous membranes, skin, thrombocytopathy, platelet dysfunction, hypocoagulation, hemorrhagic rashes (purpura), thrombophlebitis were observed.
Metabolic disorders: possible hypoglycemia (dizziness, increased sweating, headache, visual disturbances) due to improved glucose utilization.
On the part of the immune system: malaise; allergic reactions (urticaria, eczema, petechial rashes, itching, dermatitis, skin rashes) up to the development of anaphylactic shock may occur at the injection site.
Local reactions: in patients with hypersensitivity to thioctic acid, a burning sensation may occur at the injection site, which resolves spontaneously or when the rate of drug administration is reduced.
Cardiovascular system: pain in the heart area, tachycardia.
After intravenous administration, in some cases, spotty hemorrhages in the mucous membranes and skin, thrombopathies were observed. As a result of improved glucose absorption, in some cases, blood sugar levels may decrease.
After rapid intravenous administration, a feeling of tightness in the chest often occurs.
Expiration date
3 years.
The shelf life after dissolution in physiological saline solution under conditions of protection from light is 6 hours.
Storage conditions
Store at a temperature not exceeding 25 °C in the original packaging to protect from light.
Keep out of reach of children.
Incompatibility
Thioctic acid reacts in vitro with metal ion complexes (for example, with cisplatin).
Thioctic acid injection solution is incompatible with glucose solution, Ringer's solution, as well as with solutions known to react with SH groups or with disulfide bridges.
Only 0.9% sodium chloride solution should be used as a carrier solution for Espa-lipon® infusions.
Packaging
24 ml in a brown glass ampoule; 5 ampoules in a cardboard box.
Vacation category
According to the recipe.
Producer
Esparma GmbH, Germany.
Location of the manufacturer and its business address
Wallenroder Strasse 8-10, 13435 Berlin, Germany.
