Instructions for Lipothion film-coated tablets 600 mg No. 30
Composition
active ingredient: thioctic (α-lipoic) acid;
1 film-coated tablet contains 600 mg of thioctic (α-lipoic) acid;
Excipients: lactose monohydrate; colloidal anhydrous silica; simethicone; croscarmellose sodium; microcrystalline cellulose; hypromellose; magnesium stearate;
shell composition: Opadry® 200 Optimized Performance Coating 200F210038 green (polyvinyl alcohol, talc, titanium dioxide (E 171), macrogol, methacrylate copolymer dispersion, quinoline yellow (E 104), indigo carmine (E 132), sodium bicarbonate).
Dosage form
Film-coated tablets.
Main physicochemical properties: oblong biconvex tablets, coated with a yellow-green film coating.
Pharmacotherapeutic group
Drugs affecting the digestive system and metabolic processes. Thioctic acid. ATC code A16A X01.
Pharmacological properties
Pharmacodynamics.
α-Lipoic acid plays the role of a coenzyme in the oxidative decarboxylation of α-keto acids.
Hyperglycemia caused by diabetes leads to the accumulation of glucose on the matrix proteins of blood vessels and the formation of so-called “advanced glycation end products.” This process leads to reduced endoneural blood flow and endoneural hypoxia/ischemia, which is associated with increased production of oxygen free radicals, which lead to peripheral nerve damage.
Animal studies have shown that α-lipoic acid affects biochemical processes caused by streptozotocin-induced diabetes, leading to improved endoneural blood flow and increased levels of the physiological antioxidant glutathione, and as an antioxidant, it reduces the number of oxygen free radicals in the diabetically altered nerve.
The effects observed in the experiment indicate that peripheral nerve function can be improved with α-lipoic acid. This is relevant to the sensory disturbances in diabetic polyneuropathy, which can manifest in such forms of paresthesia as burning, pain, numbness, and "creeping sensations."
Pharmacokinetics.
Absorption
When administered orally, α-lipoic acid is rapidly absorbed. Due to the significant first-pass effect, the absolute bioavailability of α-lipoic acid (defined as the parent substance) when administered orally is approximately 20% compared to that when administered intravenously.
Similar to the oral solution, which is the standard dosage form for maximum absorption, α-lipoic acid tablets have an absorption profile with a rapid influx of active substance, accompanied by reduced interindividual variability. The relative bioavailability of the tablets (compared to the oral solution) is > 60%. The maximum plasma concentration of 4 μg/ml was observed approximately 0.5 hours after oral administration of 600 mg α-lipoic acid.
Biotransformation
The biotransformation of α-lipoic acid occurs mainly through oxidative reduction of side chains (β-oxidation) and/or through S-methylation of the corresponding thiols.
Breeding
Due to its rapid distribution in tissues, the half-life of α-lipoic acid is approximately 25 minutes.
Experiments on animals (rats, dogs) using radioactive labels have shown that α-lipoic acid is excreted mainly by the kidneys by 80-90%, mainly in the form of metabolites. In humans, only a small part of the unchanged substance remains in the urine.
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.
Thioctic acid should not be used simultaneously with metal compounds (iron, magnesium preparations, with dairy products, since they contain calcium), since it is a metal chelator. In the case of using the daily dose of thioctic acid 30 minutes before breakfast, preparations containing iron or magnesium should be taken at lunch or in the evening.
Thioctic acid forms poorly soluble complexes with sugar molecules (for example, with a solution of lavulose).
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.
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. The restriction also applies to breaks between courses of treatment.
Application features
After the use of thioctic acid, an unusual odor of urine may be observed; this phenomenon is not clinically significant.
At the beginning of treatment for polyneuropathy, due to regeneration processes, a short-term increase in paresthesias with a feeling of "creeping ants" is possible.
Autoimmune insulin syndrome (AIS) has been reported with the use of thioctic acid. Patients with the human leukocyte antigen genotype HLA-DRB1*04:06 and HLA-DRB1*04:03 alleles are more susceptible to the development of AIS. The HLA-DRB1*04:03 allele (sensitivity for AIS: 1.6) was particularly prevalent in Caucasians, with a higher prevalence in southern than northern Europe, and the HLA-DRB1*04:06 allele (sensitivity for AIS: 56.6) was particularly prevalent in Japanese and Korean patients. AIS should be considered in the differential diagnosis of spontaneous hypoglycemia in patients receiving the drug (see section "Adverse reactions").
The medicinal product contains lactose, therefore it should not be used in patients with rare hereditary forms of galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.
This medicinal product contains less than 1 mmol (23 mg) sodium/dose, i.e. essentially sodium-free.
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
When using the drug, caution should be exercised (due to the possibility of side effects such as dizziness and visual disturbances) when driving vehicles or engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
Method of administration and doses
The drug is intended for oral use. The tablets are taken on an empty stomach, without chewing and with sufficient water. Taking the drug during meals may reduce the absorption of thioctic acid, so it is recommended to take the entire daily dose half an hour before breakfast (the first meal).
Adults
The daily dose is 600 mg of thioctic acid (1 tablet).
The duration of treatment is determined by the doctor individually.
Children.
Since there is 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
Symptoms
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 intoxication, in some cases fatal, has been observed. At the initial stage, the clinical picture of intoxication may manifest itself in the form of psychomotor agitation or 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 cases of intoxication with high doses of thioctic acid.
Treatment
If severe intoxication is suspected (e.g. more than 10 tablets of 600 mg for adults and more than 50 mg/kg body weight for children), immediate hospitalization is recommended and measures are taken in accordance with the general principles of accidental poisoning (e.g. induce vomiting, rinse the stomach, administer activated charcoal). 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; such treatment should be symptomatic. The benefit of hemodialysis, hemoperfusion or the use of filtration methods with forced removal of thioctic acid has not yet been confirmed.
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).
On the part of the immune system:
very rarely - allergic reactions, including skin rashes, urticaria (urticaria), itching and eczema; frequency unknown - autoimmune insulin syndrome (see section "Special warnings and precautions for use").
Metabolism and nutrition:
very rarely - hypoglycemia*.
often - dizziness; very rarely - change or disturbance of taste sensations, headache*, increased sweating*.
On the part of the organs of vision:
very rarely - visual disturbances*.
From the respiratory system, chest organs and mediastinum:
difficulty breathing.
From the digestive system:
often - nausea; very rarely - gastrointestinal disorders, including vomiting, abdominal and gastrointestinal pain, diarrhea.
*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 of suspected adverse reactions.
Reporting adverse reactions after the registration of a medicinal product is important. This allows monitoring of the benefit/risk ratio when using this medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of the medicinal product via the Automated Information System for Pharmacovigilance at the link: https://aisf.dec.gov.ua.
Expiration date
3 years.
Storage conditions
Store at a temperature not exceeding 25 °C in the original packaging and out of the reach of children.
Packaging
10 tablets in a blister; 3, 6 or 10 blisters in a cardboard box.
Vacation category
According to the recipe.
Producer
WORLD MEDICINE ILACH SAN. VE TIJ. A.Sh./
WORLD MEDICINE ILAC SAN. VE TIC. AS
Location of the manufacturer and address of its place of business.
15 Temmuz Mahalleshi Cami Yolu Caddesi No. 50 Guneshli Bagcilar/Istanbul, Turkey/
15 Temmuz Mahallesi Cami Yolu Caddesi No:50 Gunesli Bagcilar/Istanbul, Turkey.
Applicant
LLC "WORLD MEDICINE", Ukraine/
WORLD MEDICINE, LLC, Ukraine.
