Instructions Dialipon capsules 300 mg blister No. 30
Composition
active ingredient: thioctic acid;
1 capsule contains 300 mg (0.3 g) of alpha-lipoic acid;
Excipients: lactose monohydrate, microcrystalline cellulose, hypromellose (E15), colloidal anhydrous silica, magnesium stearate.
Dosage form
Capsules.
Main physicochemical properties: hard gelatin capsules No. 0. The body and cap of the capsule are ivory. The contents of the capsule are a powdery, granular mixture of yellow color.
Pharmacotherapeutic group
Drugs affecting the digestive system and metabolic processes. ATX code A16A X01.
Pharmacological properties
Pharmacodynamics
Thioctic acid is an endogenous substance that has a vitamin-like effect, acts as a coenzyme and is involved in the oxidative decarboxylation of a-keto acids. As a result of hyperglycemia, which occurs in diabetes mellitus, glucose is attached to the matrix proteins of blood vessels and the so-called “end products of accelerated glycolysis” are formed. This process leads to a decrease in endoneural blood flow and endoneural hypoxia/ischemia, which, in turn, leads to an increased formation of oxygen-containing free radicals that damage peripheral nerves. A decrease in the level of antioxidants, such as glutathione, in peripheral nerves has also been noted.
Pharmacokinetics
After oral administration, thioctic acid is rapidly absorbed. As a result of significant presystemic metabolism, the absolute bioavailability of thioctic acid is approximately 20%. Due to rapid distribution in the tissues, the half-life of thioctic acid in blood plasma is approximately 25 minutes. The relative bioavailability of thioctic acid when administered orally in solid dosage forms is more than 60% in proportion to the drinking solution. The maximum plasma concentration of approximately 4 μg/ml was measured approximately 30 minutes after oral administration of 600 mg of thioctic acid. Only a small amount of the substance is found in the urine in an unchanged state. Biotransformation is carried out by oxidative reduction of the side chain (β-oxidation) and/or S-methylation of the corresponding thiols. Thioctic acid reacts in vitro with metal ion complexes, for example with cisplatin, and forms sparingly soluble complexes with sugar molecules.
Indication
Prevention and treatment of 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
The effectiveness of cisplatin is reduced when used simultaneously with Dialipon®. Thioctic acid is a metal complexing agent, and therefore, according to the basic principles of pharmacotherapy, it should not be used simultaneously with metal compounds (for example, with food supplements containing iron or magnesium, with dairy products, since they contain calcium). If the total daily dose of the drug is taken 30 minutes before breakfast, then food supplements containing iron and magnesium should be taken in the afternoon or evening.
When using thioctic acid in patients with diabetes mellitus, it is possible to enhance the hypoglycemic effect of insulin and oral antidiabetic agents, therefore, especially at the initial stage of treatment, careful monitoring of blood sugar levels is recommended. To avoid symptoms of hypoglycemia, in some cases it may be necessary to reduce the dose of insulin or oral antidiabetic agents.
Ethanol reduces the therapeutic efficacy of thioctic acid.
Application features
The main factor in the effective treatment of diabetic polyneuropathy is optimal correction of the patient's blood sugar level. At the beginning of treatment of polyneuropathy, due to regeneration processes, a short-term increase in paresthesias with a feeling of "crawling ants" is possible.
When using thioctic acid in patients with diabetes mellitus, frequent monitoring of blood glucose levels is necessary. In some cases, it is necessary to reduce the doses of antidiabetic drugs to prevent the development of hypoglycemia.
Regular consumption of alcoholic beverages is a significant risk factor for the development and progression of polyneuropathy and may interfere with treatment success, so alcohol consumption should be avoided during treatment and in the periods between courses of treatment.
Cases of autoimmune insulin syndrome (AIS) have been reported during treatment with thioctic acid. Patients with the human leukocyte antigen genotype (HLA-DRB1*04:06 and HLA-DRB1*04:03 alleles) are more prone to developing AIS during treatment with thioctic acid. The HLA-DRB1*04:03 allele (susceptibility factor for AIS development – 1.6) is particularly common in representatives of the Caucasian race (in Southern Europe more than in Northern Europe), and the HLA-DRB1*04:06 allele (susceptibility factor for AIS development – 56.6) is particularly common in Japanese and Korean patients. AIS should be considered in the differential diagnosis of spontaneous hypoglycemia in patients using thioctic acid.
Ability to influence reaction speed when driving vehicles or other mechanisms
During treatment, caution should be exercised when driving vehicles, operating other mechanisms, or engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions, due to the possibility of adverse reactions such as hypoglycemia (dizziness and visual impairment).
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. The daily dose is 600 mg of thioctic acid (2 capsules of Dialipon® 300 mg), which should be taken once 30 minutes before the first meal. The capsules should not be chewed and washed down with sufficient liquid.
In case of severe paresthesia, it is advisable to start treatment with parenteral administration of Dialipon, solution for injection, for 2–4 weeks. In the future, treatment should be continued with oral administration of the drug at a dose of 600 mg once a day.
The duration of treatment is determined by the doctor depending on the nature and course of the disease.
Children
The drug should not be prescribed to children, as there is insufficient clinical experience in this age group.
Overdose
Overdose may cause nausea, vomiting and headache. After accidental ingestion or attempted suicide with oral administration of thioctic acid in doses from 10 g to 40 g in combination with alcohol, significant intoxications, in some cases fatal, have been observed. At the initial stage, the clinical picture of intoxication may manifest itself in psychomotor agitation or impaired consciousness. Generalized convulsions and lactic acidosis then occur. In addition, hypoglycemia, shock, acute skeletal muscle necrosis, hemolysis, disseminated intravascular coagulation syndrome, bone marrow suppression and multiple organ failure have been described in intoxication with large doses of thioctic acid.
Treatment. Even if severe intoxication with Dialipon® is suspected (e.g., ingestion of more than 20 capsules of 300 mg for adults or a dose of more than 50 mg/kg of body weight for children), immediate hospitalization and the use of measures in accordance with the general principles of accidental poisoning (e.g., induce vomiting, gastric lavage, use activated charcoal) are recommended. Symptomatic treatment of generalized convulsions, lactic acidosis and other life-threatening consequences of intoxication should be carried out in accordance with the principles of modern intensive care. At present, the benefit of hemodialysis, hemoperfusion or filtration methods with forced removal of thioctic acid has not been confirmed.
Adverse reactions
Classification of the frequency of adverse reactions:
very common: ≥ 1/10;
common: ≥ 1/100 - <1/10;
uncommon: ≥ 1/1000 - < 1/100;
rare: ≥ 1/10,000 – < 1/1,000;
very rare: <1/10,000;
not known: frequency cannot be estimated from the available data.
From the nervous system
Very rare: change or disturbance of taste sensations.
From the digestive tract
Common: nausea.
Very rare: vomiting, abdominal and gastrointestinal pain, diarrhea.
Metabolic
Very rare: decreased blood sugar levels. There have been reports of complaints suggestive of hypoglycaemic states, such as dizziness, increased sweating, headache and visual disturbances.
On the part of the immune system
Very rare: allergic reactions, including skin rashes, hives (urticaria), itching, difficulty breathing.
Not known: autoimmune insulin syndrome.
Others
Not known: eczema.
Expiration date
2 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.
Packaging
10 capsules in a blister. 3 blisters in a pack.
Vacation category
According to the recipe.
Producer
JSC "Farmak".
Location of the manufacturer and its business address
Ukraine, 04080, Kyiv, Kyrylivska St., 74.
