Instructions Dialipon solution for infusions 3% ampoule 20 ml No. 5
Composition
active ingredient: thioctic acid;
1 ml of solution contains 58.382 mg of meglumine salt of alpha-lipoic acid, which, when calculated per 100% substance, corresponds to 30 mg of alpha-lipoic acid;
excipients: meglumine (N-methylglucamine), polyethylene glycol 300 (macrogol 300), water for injections.
Dosage form
Solution for infusion.
Main physicochemical properties: clear yellow liquid.
Pharmacotherapeutic group
Drugs affecting the digestive system and metabolic processes. ATC code A16A X01.
Pharmacological properties
Pharmacodynamics
Thioctic acid is a substance similar to vitamins, but which 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 depletion of such an antioxidant as glutathione in peripheral nerves. In studies on rats, thioctic acid thus influenced the biochemical process caused by diabetes mellitus, which was provoked by streptozotocin, which reduced the formation of advanced glycosylation end products, 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 on free radicals. These effects observed in the experiment indicate that thioctic acid can improve the function of peripheral nerves. This applies to sensory disorders that occur in polyneuropathy and can manifest themselves in the form of dysesthesias, paresthesias, such as, for example, a burning sensation, pain, a feeling of numbness or "creeping". A study aimed at studying the effectiveness of thioctic acid for the symptomatic treatment of diabetic polyneuropathy confirmed the data on the beneficial effects of thioctic acid on such studied symptoms as paresthesia, burning sensation, numbness, and pain.
Pharmacokinetics
Thioctic acid is highly subject to the first-pass effect through the liver. There are significant individual fluctuations in systemic bioavailability. Thioctic acid is biotransformed by side-chain oxidation and conjugation, and 80-90% of its metabolites are excreted by the kidneys. The half-life of thioctic acid is 25 minutes, and the total plasma clearance is 10-15 ml/min/kg. After a 30-minute infusion of 600 mg of thioctic acid, its plasma content is about 20 μg/ml. Only a small amount of the excreted intact substance is found in the urine.
Indication
Paresthesia in diabetic polyneuropathy.
Contraindication
Hypersensitivity to thioctic acid or to any other component 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 (iron, magnesium preparations).
Thioctic acid may enhance the blood sugar-lowering effect of insulin and/or other antidiabetic agents, therefore, especially at the beginning of treatment with thioctic acid, regular monitoring of blood sugar levels is indicated. 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.
Application features
In the treatment of patients with diabetes mellitus, frequent glycemic control is necessary. In some cases, it is necessary to adjust the doses of sugar-lowering drugs 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."
Chronic alcohol consumption is a risk factor for polyneuropathy and may reduce the effectiveness of Dialipon®. Therefore, it is recommended to abstain from alcohol during treatment with the drug.
The drug is light-sensitive, so ampoules should be removed from the packaging only immediately before use.
A certain limitation of intravenous administration of thioctic acid preparations is old age (over 75 years).
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.
Ability to influence reaction speed when driving vehicles or other mechanisms
When using the drug, caution must be exercised when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.
Method of administration and doses
The dose and duration of treatment are determined by the doctor individually.
In case of intense paresthesias, intravenous administration of the drug is recommended at a dose of 10 ml to 20 ml per day, which corresponds to 300-600 mg of thioctic acid per day. The infusion solution should be used for 2-4 weeks at the initial stage of treatment. The contents of the ampoule should be diluted in 250 ml of 0.9% sodium chloride solution and administered intravenously, with the infusion duration being at least 30 minutes. Due to the sensitivity of the active substance to light, the infusion solution should be prepared immediately before administration and protected from light, for example with aluminum foil. The prepared infusion solution can be stored for 6 hours if protected from light.
For further therapy, use oral forms of the drug DialiponÒ at a dose of 300-600 mg of thioctic acid per day.
Children
Dialipon® is not recommended for use in children and adolescents due to the lack of clinical experience with the use of the drug in this category of patients.
Overdose
Overdose may cause nausea, vomiting and headache. When using very high doses of 10 to 40 g of thioctic acid in combination with alcohol, severe intoxication is observed, which can be fatal. The clinical picture of poisoning is initially manifested by psychomotor agitation or impaired consciousness and subsequently proceeds with attacks of generalized convulsions and the development of lactic acidosis. The consequences of intoxication may be hypoglycemia, shock, rhabdomyolysis, hemolysis, disseminated intravascular coagulation, bone marrow suppression and multiorgan failure.
Treatment. If significant intoxication is suspected (> 80 mg/kg body weight of thioctic acid), immediate hospitalization and implementation of generally accepted measures (e.g., induced vomiting, gastric lavage, use of activated charcoal) are indicated. Treatment of generalized convulsive attacks, lactic acidosis and other life-threatening consequences of intoxication should be guided by modern principles of intensive care and carried out symptomatically. To date, there is no data on the feasibility of using hemodialysis, hemoperfusion or hemofiltration methods within the framework of forced removal of thioctic acid.
Adverse reactions
Central nervous system: change or disturbance of taste sensations, headache, hot flashes, increased sweating, difficulty breathing, increased intracranial pressure, dizziness, convulsions, visual disturbances and double vision. In most cases, all of these manifestations resolve on their own.
On the part of the digestive tract: with rapid intravenous administration of the drug, nausea, vomiting, diarrhea, abdominal pain were observed, which resolved on their own.
From the side of the hematopoietic system: petechial hemorrhages in the mucous membranes/skin, platelet dysfunction, hypocoagulation, hemorrhagic rash (purpura), thrombophlebitis.
Metabolic disorders: due to improved glucose absorption, in some cases blood sugar levels may decrease, which may cause symptoms similar to hypoglycemia, such as dizziness, increased sweating, headache, and visual disturbances.
On the part of the immune system: skin rashes, urticaria, itching, eczema, as well as systemic reactions up to the development of anaphylactic shock.
Cardiovascular system: with rapid intravenous administration, pain in the heart area and tachycardia may occur, which resolve spontaneously.
Other: injection site reactions, weakness.
Expiration date
5 years.
Do not use the drug after the expiration date indicated on the package.
Storage conditions
Store in original packaging at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Incompatibility
Dialipon® reacts in vitro with metal ion complexes (e.g. cisplatin), so the drug may reduce their effect. Dialipon® forms poorly soluble complex compounds with sugars. Therefore, the infusion solution of Dialipon® is incompatible with glucose, fructose, Ringer's solution. The drug is incompatible with solutions containing compounds that react with SH-groups or disulfide bridges. Use only 0.9% sodium chloride solution to dilute the drug.
Packaging
10 ml or 20 ml in an ampoule; 5 or 10 ampoules in a pack.
5 ampoules in a blister; 1 or 2 blisters in a pack.
Vacation category
According to the recipe.
Producer
PJSC "Farmak".
Location
Ukraine, 04080, Kyiv, Frunze St., 63.
