Instructions Thioctacid 600 HR film-coated tablets 600 mg bottle No. 30
Composition
active ingredient: thioctic acid (thioctic (α-lipoic) acid);
1 film-coated tablet contains 600 mg of thioctic (α-lipoic) acid;
excipients: low-substituted hydroxypropylcellulose, hydroxypropylcellulose, magnesium stearate, hypromellose, macrogol 6000, titanium dioxide (E 171), talc, quinoline yellow (E 104), indigo carmine (E 132).
Dosage form
Film-coated tablets.
Main physicochemical properties: yellow-green with a matte sheen, biconvex, oblong tablets, coated.
Pharmacotherapeutic group
Drugs that affect the digestive system and metabolic processes. Thioctic acid.
ATX 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 the 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 forms of paresthesia such as burning, pain, numbness, and "creeping sensations."
Pharmacokinetics
When Thioctacid® 600 HR is administered orally (rapid release), 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 taking Thioctacid® 600 HR tablets is approximately 20% compared to that after intravenous administration. Due to the rapid distribution in the tissues, the half-life of α-lipoic acid is approximately 25 minutes. Like the oral solution, which is the standard dosage form with maximum absorption, Thioctacid® 600 HR tablets have an absorption profile with a rapid influx of the active substance, which is accompanied by a decrease in interindividual variability. The relative bioavailability of Thioctacid® 600 HR (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 of α-lipoic acid. Experiments on animals (rats, dogs) using radioactive labels showed that the drug 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. Biotransformation occurs mainly due to oxidative reduction of side chains (β-oxidation) and/or by S-methylation of the corresponding thiols.
Indication
Treatment of symptoms of peripheral (sensorimotor) diabetic polyneuropathy.
Contraindication
Hypersensitivity to thioctic acid and other components of the drug.
Interaction with other medicinal products and other types of interactions
Thioctic acid is a metal chelator, so it cannot be used together with metal compounds (iron, magnesium preparations, with dairy products, since they contain calcium). If the daily dose of the drug is used 30 minutes before breakfast, then preparations containing iron or magnesium should be used at lunch or in the evening. α-lipoic acid forms poorly soluble complexes with sugar molecules (for example, with a solution of lavulose).
When using Thioctacid® 600 HR 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.
WARNING
Regular alcohol consumption is a significant risk factor for the development and progression of the clinical picture of neuropathy and may therefore negatively affect the treatment process with Thioctacid® 600 HR. Therefore, patients with diabetic polyneuropathy are usually advised to abstain from alcohol whenever possible. Limiting alcohol consumption also applies to breaks between courses of treatment.
Application features
When using the drug, an unusual urine odor may be observed, which has no clinical significance.
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.
Ability to influence reaction speed when driving vehicles or other mechanisms
During treatment, caution should be exercised (due to the possibility of side effects such as dizziness and visual disturbances) 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 prescribed 1 tablet of Thioctacid® 600 HR (equivalent to 600 mg of α-lipoic acid) once a day. Take approximately half an hour before the first meal.
The drug is taken on an empty stomach, without chewing and with sufficient water. Taking the drug during meals may reduce the absorption of α-lipoic acid, so it is recommended to take the entire daily dose half an hour before breakfast.
The duration of treatment is determined by the doctor individually.
Children
Since there is no data on the safety and effectiveness of this drug in children, it is not recommended to prescribe the drug to this age group of patients.
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 intoxication was observed, in some cases with a fatal outcome. 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 intoxication with high doses of thioctic acid.
Treatment. If severe intoxication with the drug is suspected, 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.
Adverse reactions
On the part of the digestive tract: often - nausea; in rare cases - gastrointestinal disorders, including vomiting, abdominal pain and gastrointestinal pain, diarrhea.
Allergic reactions: in rare cases - allergic reactions, including skin rashes, hives (urticaria), itching and eczema.
From the side of the central nervous system: often - dizziness; very rarely - change or disturbance of taste sensations.
Metabolic disorders: in isolated cases - a decrease in blood sugar levels. There have been reports of complaints indicating hypoglycemic states (dizziness, increased sweating, headache and visual disturbances).
Others: difficulty breathing.
Expiration date
5 years.
Storage conditions
Store at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Packaging
30 film-coated tablets in a bottle.
Vacation category
According to the recipe.
Producer
MEDA Pharma GmbH & Co. KG.
Location of the manufacturer and its business address
Benzstrasse 1, 61352 Bad Homburg, Germany.
