Instructions Alpha-Lipon film-coated tablets 600 mg blister No. 30
Composition
active ingredient: 1 tablet contains 300 mg or 600 mg of alpha-lipoic (thioctic) acid;
excipients: lactose, monohydrate; microcrystalline cellulose; croscarmellose sodium; corn starch; sodium lauryl sulfate; colloidal anhydrous silica; magnesium stearate; shell: Opadry II Yellow film-coating mixture (lactose, monohydrate; hypromellose (hydroxypropylmethylcellulose); polyethylene glycol (macrogol); indigotine (E 132); sunset yellow FCF (E 110); quinoline yellow (E 104); titanium dioxide (E 171); triacetin).
Dosage form
Film-coated tablets.
Main physicochemical properties:
300 mg: round tablets with a biconvex surface, coated with a yellow film coating;
600 mg: oblong tablets with a biconvex surface, scored on both sides, coated with a yellow film coating.
Pharmacotherapeutic group
Drugs affecting the digestive system and metabolic processes. ATX code A16A X01.
Pharmacological properties
Pharmacodynamics.
Thioctic acid is an endogenous vitamin-like substance that acts as a coenzyme and participates in the oxidative decarboxylation of α-keto acids. As a result of hyperglycemia, which occurs in diabetes mellitus, glucose is attached to the matrix proteins of blood vessels and the formation of so-called "advanced glycation end products". 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 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
Paresthesia in diabetic polyneuropathy.
Contraindication
Hypersensitivity to thioctic acid or to any of the components of the drug.
Interaction with other medicinal products and other types of interactions
The effectiveness of cisplatin is reduced when used simultaneously with the drug Alpha-lipoic acid. 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 middle of the day or in the evening. When using thioctic acid in patients with diabetes mellitus, the blood sugar-lowering effect of insulin and oral antidiabetic agents may be enhanced, therefore, especially at the initial stage of treatment, careful monitoring of blood sugar levels is recommended. In order to avoid symptoms of hypoglycemia, in some cases, a reduction in the dose of insulin or oral antidiabetic agents may be required.
Application features
At the beginning of treatment of polyneuropathy due to regenerative 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.
The drug Alpha-Lipon contains lactose, so it should not be used in patients with rare hereditary diseases such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome. The dye E 110, which is part of the tablet shell, may cause allergic 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.
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).
Method of administration and doses
The daily dose is 600 mg of thioctic acid (2 tablets of 300 mg or 1 tablet of 600 mg), which should be taken as a single dose 30 minutes before the first meal. Simultaneous food intake makes absorption difficult, so it is especially important for patients with prolonged gastric emptying to take the medicine before meals. The tablets should not be chewed and should be washed down with a sufficient amount of liquid, for example, 1 glass of water.
In case of intense paresthesia, treatment can be started with parenteral administration of thioctic acid, using appropriate dosage forms.
Children
Alpha-lipoic acid should not be administered to children, as there is insufficient clinical experience in this age group.
Overdose
Symptoms: Overdose may cause nausea, vomiting and headache. After accidental use 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 in clouding of consciousness. Later, generalized convulsions and lactic acidosis 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 high doses of thioctic acid.
Treatment. Even if severe intoxication with Alpha-Lipon is suspected (e.g., use of more than 20 tablets of 300 mg for adults or a dose of more than 50 mg/kg of body weight in children), immediate hospitalization and measures for accidental poisoning (e.g., induction of vomiting, gastric lavage, use of activated charcoal) are recommended. Treatment of generalized convulsions, lactic acidosis and other life-threatening consequences of intoxication should be symptomatic and should be carried out in accordance with the principles of modern intensive care. The benefit of hemodialysis, hemoperfusion, or filtration methods with forced removal of thioctic acid has not been confirmed to date.
Adverse reactions
From the nervous system: change or disturbance of taste sensations.
Gastrointestinal: nausea, vomiting, abdominal and gastrointestinal pain, diarrhea.
Metabolic: decreased blood sugar levels. There have been reports of complaints suggestive of hypoglycemic states, namely dizziness, increased sweating, headache and visual disturbances.
On the part of the immune system: allergic reactions, including skin rashes, hives (urticaria), itching, difficulty breathing.
Other: eczema (frequency cannot be estimated from the available data).
Expiration date
2 years.
Storage conditions
Store in the original packaging at a temperature not exceeding 25 ºС.
Keep out of reach of children.
Packaging
For a dose of 300 mg. 10 tablets in a blister; 3 blisters in a pack.
For a dose of 600 mg. 6 tablets in a blister; 5 blisters in a pack.
10 tablets in a blister; 3 or 6 blisters in a pack.
Vacation category
According to the recipe.
Producer
PJSC "Kyiv Vitamin Plant".
Location of the manufacturer and its business address
04073, Ukraine, Kyiv, Kopylivska St., 38.
