Thioctic acid

Pharmacological properties

Thioctic acid is an endogenous vitamin-like substance that acts as a coenzyme and takes part in the oxidative decarboxylation of α-keto acids. due to hyperglycemia that occurs in diabetes mellitus, glucose joins the matrix proteins of blood vessels and the formation of the so-called end products of accelerated glycolization. this process leads to a decrease in endoneural blood flow and endoneural hypoxia / ischemia, which, in turn, leads to increased formation of oxygen-containing free radicals that damage peripheral nerves. there has also been a decrease in the level of antioxidants, such as glutathione, in the peripheral nerves.

Pharmacokinetics After oral administration, thioctic acid is rapidly absorbed. As a result of significant presystemic metabolism, the absolute bioavailability of thioctic acid is about 20%. Due to the rapid distribution in the tissues, the half-life of thioctic acid in the blood plasma is about 25 minutes. The relative bioavailability of thioctic acid during oral administration of solid dosage forms is more than 60% in proportion to the drinking solution. C_max in plasma about 4 μg / ml was reached approximately 30 minutes after oral administration of 600 mg of thioctic acid. In urine, only a small amount of the substance is determined unchanged. Biotransformation is carried out due to oxidative reduction of the side chain (β-oxidation) and / or S-methylation of the corresponding thiols. In vitro thioctic acid reacts with metal ion complexes, such as cisplatin, and forms moderately soluble complexes with sugar molecules.

Indications

Paresthesia in diabetic polyneuropathy.

Application

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 ingestion complicates absorption, therefore, patients who are characterized by prolonged emptying of the stomach, it is especially important to use the drug before eating. do not chew the tablets and drink with a sufficient amount of liquid, for example, 1 glass of water.

With intense paresthesias, treatment can be started with parenteral administration of thioctic acid using the appropriate dosage forms.

Contraindications

Hypersensitivity to thioctic acid or any of the components of the drug.

Side effects

From the nervous system: a change or violation of taste sensations.

From the gastrointestinal tract: nausea, vomiting, abdominal pain and gastrointestinal pain, diarrhea.

On the part of metabolism: a decrease in blood glucose. There have been reports of complaints indicating hypoglycemic conditions, namely, dizziness, increased sweating, headache, and visual impairment.

From the immune system: allergic reactions, including skin rash, urticaria (urticaria rash), itching, shortness of breath.

Others: eczema (assessment of the incidence cannot be carried out according to available data).

special instructions

At the beginning of the treatment of polyneuropathy due to regenerative processes, a short-term increase in paresthesia with the sensation of "creeping crawl" is possible. when using thioctic acid in patients with diabetes, frequent monitoring of blood glucose levels is necessary. in some cases, it is necessary to reduce the dose 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 impede treatment success, therefore, alcohol should be avoided during treatment and between treatment courses.

The drug Alpha-lipon contains lactose, so it should not be used in patients with rare inherited diseases such as galactose intolerance, lactase deficiency or glucose-galactose malabsorption syndrome.The dye E110, which is part of the tablet shell, can cause allergic reactions.

Use during pregnancy and lactation. 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, so it is not recommended to use it during lactation.

Children. Alpha-lipon should not be prescribed to children, since there is no sufficient clinical experience for this age category.

The ability to influence the reaction rate when driving vehicles and working with other mechanisms. During treatment, care must be taken when driving vehicles, other mechanisms, or engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions, because of the possibility of adverse reactions such as hypoglycemia (dizziness and visual impairment).

Interactions

The effectiveness of cisplatin decreases with the simultaneous use of alpha-lipon with the drug. thioctic acid is a complexing agent of metals and therefore, according to the basic principles of pharmacotherapy, it should not be used simultaneously with metal compounds (for example, with food additives containing iron or magnesium, with dairy products, since they contain calcium). if the total daily dose of the drug is used 30 minutes before breakfast, then nutritional supplements containing iron and magnesium should be used in the middle of the day or in the evening. when thioctic acid is used in patients with diabetes, the hypoglycemic effect of insulin and oral antidiabetic agents may be enhanced, therefore, especially at the initial stage of treatment, careful monitoring of blood glucose 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.

Overdose

Symptoms: with an overdose, nausea, vomiting, and headache may occur. after accidental use or when attempting suicide with oral administration of thioctic acid in doses of 10–40 g in combination with alcohol, significant intoxication was noted, in some cases fatal.

At the initial stage, the clinical picture of intoxication can manifest itself in psychomotor agitation or blurred consciousness. In the future, generalized convulsions and lactic acidosis occur. In addition, during intoxication with high doses of thioctic acid, hypoglycemia, shock, acute skeletal muscle necrosis, hemolysis, disseminated intravascular coagulation, inhibition of bone marrow activity and multiple organ failure were described.

Treatment. Even if you suspect severe drug intoxication, Alpha-lipon (for example, the use of more than 20 tablets of 300 mg for adults or a dose of more than 50 mg / kg body weight in children), immediate hospitalization and measures to be taken in case of accidental poisoning (for example, inducing vomiting, gastric lavage , the use of activated carbon). Treatment of generalized seizures, lactic acidosis and other life-threatening intoxication effects should be symptomatic, it should be carried out in accordance with the principles of modern intensive care. So far, the benefits of hemodialysis, hemoperfusion or filtration methods with the forced elimination of thioctic acid have not been confirmed.

Storage conditions

In the original packaging at a temperature not exceeding 25 ° C.