Thioctic acid-Vial - instructions for use, dose, side effects, contraindications

Excipients: cellulose microcrystalline - 264.76 mg, corn starch - 86.00 mg, sodium carboxymethyl starch (type A) - 12.00 mg, povidone K-30 - 10.00 mg, croscarmellose sodium 8.00 mg, magnesium stearate-6 , 80 mg, talc-6.60 mg, silicon colloidal dioxide 5.00 mg, methyl parahydroxybenzoate 0.70 mg, propyl parahydroxybenzoate 0.14 mg.

Shell

White film coating Color Coat FC4S-H (hypromellose 15 cP - 11.10 mg, titanium dioxide - 3.40 mg, dibutyl sebacate - 3.13 mg, hypromellose 5 cps - 2.19 mg, silicon dioxide colloid - 1.30 mg, talc - 0.88 mg) - 22.00 mg.

Dosage 600 mg

Core

Active substance: thioctic acid 600.00 mg.

Excipients: cellulose microcrystalline - 168.12 mg, corn starch - 41.70 mg, sodium carboxymethyl starch (type A) 20.00 mg, povidone K-30 - 13.35 mg, croscarmellose sodium 12.00 mg, magnesium stearate 8 , 70 mg, talc - 8.35 mg, silicon dioxide colloid - 6.70 mg, methyl parahydroxybenzoate - 0.90 mg, propyl parahydroxybenzoate - 0.18 mg.

Shell

White film coating Color Coat FC4S-H (hypromellose 15 cP - 13.54 mg, titanium dioxide - 3.35 mg, dibutyl sebacate - 3.78 mg, hypromellose 5 cps - 2.72 mg, silicon dioxide colloid -1.65 mg, talc 0.96 mg) - 26.00 mg.

Description:

Dosage of 300 mg

Round biconvex tablets covered with a film coating of white or almost white color, with a risk on one side, slight surface roughness is allowed; on the fracture, the core is seen from light yellow to light yellow with a beige tinge, white and almost white inclusions are allowed along with impregnations of a darker color.

Dosage 600 mg

Oval biconvex tablets covered with a film coating of white or almost white color, with a risk on one side, slight surface roughness is allowed; on the fracture, the core is seen from light yellow to light yellow with greenisha shade of color, white and almost white inclusions are allowed along with impregnations of a darker color.

Pharmacotherapeutic group:Metabolic means

ATX: & nbsp

A.16.A.X.01 Thioctic acid

Pharmacodynamics:Thioktovaya (alpha-lipoic) acid is an endogenous antioxidant of direct (binds free radicals) and indirect action. It is a coenzyme of the reactions of decarboxylation of alpha-keto acids. It helps to reduce the concentration of glucose in the blood plasma and increase the concentration of glycogen in the liver, also reduces insulin resistance, participates in the regulation of carbohydrate and lipid metabolism, stimulates the exchange of cholesterol. Due to its antioxidant properties, thioctic acid protects cells from damage by their decay products, reduces the formation of end products of progressive glycosylation of proteins in nerve cells in diabetes mellitus, improves microcirculation and endoneural blood flow, increases the physiological content of glutathione antioxidant. By contributing to a decrease in the concentration of glucose in the blood plasma, it affects the alternative glucose metabolism in diabetes mellitus,reduces the accumulation of pathological metabolites in the form of polyols, and, thereby, reduces edema of the nervous tissue. Due to the participation in the metabolism of fats, the hyoctic acid increases the biosynthesis of phospholipids, in particular phosphoinositides, thereby improving the damaged structure of the cell membranes; normalizes the energy exchange and the conduct of nerve impulses. Thioctic acid eliminates the toxic effect of alcohol metabolites (acetaldehyde, pyruvic acid), reduces excessive formation of molecules of free oxygen radicals, reduces endoneural hypoxia and ischemia, weakening manifestations of non-linearity in the form of paresthesia, burning sensation, pain and numbness of the limbs.
In this way, thioctic acid has antioxidant, neurotrophic, hypoglycemic action, improves lipid metabolism.

Pharmacokinetics:

Absorption and distribution

When ingested quickly and fully absorbed in the gastrointestinal tract, taking with food simultaneously reduces absorption. The time to reach the maximum concentration is 40-60 minutes. Has the effect of "first pass" through the liver. Bioavailability is 30%. The volume of distribution is about 450 ml / kg.The total plasma clearance is 10-15 ml / min.

Metabolism and excretion

Metabolized in the liver by side chain oxidation and conjugation.

Thioctic acid and its metabolites are excreted by the kidneys (80-90%). The elimination half-life is 25 minutes.

Indications:

Diabetic polyneuropathy, alcoholic polyneuropathy.

Contraindications:

Hypersensitivity to thioctic acid and any of the excipients of the drug.

Pregnancy, the period of breastfeeding (there is insufficient experience of the drug).

Children under 18 years of age (efficacy and safety of use not installed).

Carefully:

Pregnancy and lactation:

The use of thioctic acid during pregnancy is contraindicated due to the lack of sufficient experience of use.

Reproductive toxicity studies did not reveal any risks to the impact on fetal development and any embryotoxic properties of the drug.

It is not known whether the thioctic acid in mother's milk. If you need to use the drug during breastfeeding, breastfeeding should be discontinued.

Dosing and Administration:

Apply inside 600 mg once a day.

Tablets are taken on an empty stomach, approximately 30 minutes before the first meal, without chewing and washing down with sufficient water. Treatment is started after a 2-4 week course of parenteral administration.

The maximum course of taking the drug is 3 months. In some cases, taking the drug involves a longer application, the timing of which is determined by the attending physician.

Side effects:

The incidence of side effects is aligned with the WHO classification: Often 1/10); often 1/100 to <1/10); infrequently 1/1000 to <1/100); rarely (> 1/10000 to <1/1000); rarely (< 1/10000).

From the gastrointestinal tract: often - nausea; rarely - heartburn, vomiting, diarrhea, abdominal pain.

From the immune system: very rarely - allergic reactions - urticaria, skin rash, itching; systemic allergic reactions (up to the development of anaphylactic shock); frequency unknown - autoimmune insulin syndrome in patients with diabetes mellitus, which is characterized by frequent hypoglycemia in the presence of autoantibodies to insulin.

From the skin and subcutaneous tissues: the frequency is unknown - eczema.

From the nervous system: often - dizziness; rarely - change of taste sensations.

From the side of metabolism and nutrition: very rarely from- development of hypoglycemia (in connection with improvement of glucose utilization), symptoms of which include dizziness, increased sweating, headache, and visual disturbances.

Overdose:

Symptoms: headache, nausea, vomiting.

In case of acute overdose (with application of 10-40 g), serious signs of intoxication can be noted (generalized convulsive seizures, severe acid-base balance disturbances leading to lactic acidosis, hypoglycemic coma, severe bleeding disorders, sometimes leading to fatal outcome).

If you suspect a significant overdose of the drug (doses equivalent to more than 10 tablets for an adult or more than 50 mg / kg of body weight for a child), immediate hospitalization is necessary.

Treatment: symptomatic (including gastric lavage, reception of activated charcoal), if necessary - anticonvulsant therapy, measures to maintain vital functions. There is no specific antidote. Hemodialysis is not effective.

Interaction:

With the simultaneous use of thioctic acid and cisplatin, there is a decrease in the effectiveness of cisplatin.

Thioctic acid binds metals, so it should not be used simultaneously with preparations containing metals (such as iron, magnesium, calcium), as well as dairy products (because of the calcium content in them); the interval between taking such drugs and thioctic acid should be at least 2 hours.

With the simultaneous use of thioctic acid and insulin or oral hypoglycemic drugs, their effect may be enhanced.

Thioctic acid enhances the anti-inflammatory effect of glucocorticosteroids. Ethanol and its metabolites weaken the action of thioctic acid.

Special instructions:

Drinking alcohol reduces the effectiveness of drug treatment, so patients in the period drug therapy Thioctic acid should refrain from drinking alcohol throughout the course of treatment, and, if possible, in between courses. The use of alcohol during treatment with thioctic acid is also a risk factor for the development and progression of neuropathy.

Patients with diabetes require constant monitoring of blood glucose concentrations, especially at the initial stage of therapy. In some cases, it is necessary to reduce the dose of insulin or an oral hypoglycemic drug in order to avoid the development of hypoglycemia.

Simultaneous food intake can interfere with the absorption of thioctic acid.

When taking the drug, the use of dairy products is not recommended (due to the content of calcium in them). The interval between the intake of thioctic acid and the use of dairy products should be at least 2 hours.

Several cases of autoimmune insulin syndrome development in patients with diabetes mellitus have been described against thioctic acid therapy, which was characterized by frequent hypoglycemia in the presence of autoantibodies to insulin. The possibility of developing an autoimmune insulin syndrome is determined by the presence in patients of haplotypes HLA-DRB1 * 0406 and HLA-DRB1 *0403.

Effect on the ability to drive transp. cf. and fur:

The effect on the ability to drive vehicles and mechanisms has not been specially studied. Care must be taken when driving vehicles and engaging in potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

The film-coated tablets are 300 mg and 600 mg.

Packaging:

50 or 60 tablets per container polymer with a screw cap; 1 container, together with instructions for use in a pack of cardboard.

For 10 tablets in a PVC blister / aluminum foil; by 1,2, 3, 4, 5, 6, 7, 8, 9, 10 blisters are placed in a cardboard pack together with instructions for use.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-004094

Date of registration:23.01.2017

Expiration Date:23.01.2022

The owner of the registration certificate:VIAL, LLC VIAL, LLC Russia

Manufacturer: & nbsp

PROTECH BIOSYSTEMS, PVT. Ltd. India

Representation: & nbspVIAL, LLCVIAL, LLC

Information update date: & nbsp06.02.2017

Illustrated instructions

Instructions

Thioctic acid-Vial (Thioctic acid-Vial)