Thiolepta
Tiolepta: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. Drug interactions
- 12. Analogs
- 13. Terms and conditions of storage
- 14. Terms of dispensing from pharmacies
- 15. Reviews
- 16. Price in pharmacies
Latin name: Thiolepta
ATX code: A16AX01
Active ingredient: thioctic acid (acidum thiocticum)
Producer: DEKO Company, LLC (Russia), FIRM FERMENT, LLC (Russia)
Description and photo update: 2018-24-10
Prices in pharmacies: from 148 rubles.
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Thiolepta is a metabolic drug.
Release form and composition
Dosage forms of release of Tiolepta:
- solution for infusion: light yellow, with or without a greenish tinge, transparent liquid (in vials of 25 or 50 ml, in a cardboard box of 1, 3, 5 or 10 vials);
- tablets, film-coated, 0.3 g each: biconvex, round, brownish-yellow (in blister strip packs of 10 or 15 pcs., in a cardboard box 1, 3, 5, 6, 9 or 10 packs of 10 pcs. or 2, 4, 6 or 8 packs of 15 pcs.);
- tablets, film-coated, 0.6 g each: oval, brownish-yellow (in a blister strip of 10 or 15 pcs., in a cardboard box 3 or 6 packs of 10 pcs. or 2 or 4 packs of 15 pcs.).
Composition of 1 ml of Thiolept solution:
- active substance: thioctic acid (alpha-lipoic acid) - 0.012 g;
- auxiliary components: water for injection, povidone (Kollidon 17 PF or Plasdon S-15), macrogol (polyethylene glycol 400), meglumine (PM-methyl-O-glutamine).
Composition of 1 tablet Thiolepta:
- active substance: thioctic acid (alpha lipoic acid) - 0.3 or 0.6 g;
- auxiliary components: potato starch - 0.013 7 or 0.027 4 g; colloidal silicon dioxide (aerosil) - 0.013 8 or 0.027 6 g; croscarmellose sodium - 0.024 8 or 0.049 6 g; lactose monohydrate - 0.116 or 0.232 g; calcium stearate - 0.015 5 or 0.031 g; povidone K-30 - 0.032 6 or 0.065 2 g; microcrystalline cellulose - 0.083 6 or 0.167 2 g;
- shell: yellow opadry - 0.02 or 0.04 g, including hypromellose (hydroxypropyl methylcellulose) - 0.000 68 or 0.001 36 g; hyprolose (hydroxypropyl cellulose) - 0.007 or 0.013 6 g; titanium dioxide - 0.005 37 or 0.010 74 g; iron dye yellow oxide 0.000 826 or 0.001 652 g, sunset yellow dye - 0.000 004 or 0.000 008 g.
Pharmacological properties
Pharmacodynamics
Thiolepta's active ingredient, thioctic acid (alpha-lipoic acid), is an endogenous antioxidant that binds free radicals, which is formed in the body through oxidative decarboxylation of alpha-keto acids. It takes part in the oxidative decarboxylation of pyruvic acid and alpha-keto acids as a coenzyme of mitochondrial multienzyme complexes. Its biochemical action is similar in nature to the B vitamins.
Actions of Thiolepta due to thioctic acid:
- hypoglycemic, hypocholesterolemic, hypolipidemic, hepatoprotective effect;
- a decrease in blood glucose and an increase in glycogen in the liver, as well as a decrease in insulin resistance;
- regulation of carbohydrate and lipid metabolism;
- stimulation of cholesterol metabolism;
- improvement of liver function, trophism of neurons.
The use of meglumine salt of thioctic acid, which has a neutral reaction, can reduce the severity of side effects.
Pharmacokinetics
Pharmacokinetic characteristics of thioctic acid:
- absorption: the time to reach the maximum concentration - 10-11 minutes; AUC (area under the concentration-time curve) is approximately 5 μg / hr per ml; bioavailability is 30%; the substance has the effect of the first passage through the liver;
- metabolism: occurs by the liver through side chain oxidation and conjugation;
- distribution: the volume of distribution is approximately 450 ml per 1 kg; total plasma clearance - 10-15 ml per minute;
- excretion: thioctic acid and its metabolites are eliminated by 80–90% by the kidneys; the half-life varies from 20 to 50 minutes.
Indications for use
- diabetic polyneuropathy;
- alcoholic polyneuropathy.
Contraindications
- glucose-galactose malabsorption, lactase deficiency, lactose intolerance (for tablets);
- age under 18;
- pregnancy;
- period of breastfeeding;
- individual intolerance to the components contained in Tiolept.
Instructions for use of Tiolepta: method and dosage
Solution for infusion
Thiolept's solution is administered intravenously (iv) by drop, slowly, no more than 0.05 g per 1 min. The use of a perfuser is allowed, while the duration of administration should be at least 12 minutes.
When using the drug, the vials containing the solution are placed in the attached hanging black polyethylene light-shielding cases.
In cases of severe forms of alcoholic and diabetic polyneuropathy, 0.6 g of the solution is injected intravenously once a day. At the beginning of therapy, Tiolepta is administered intravenously for 14-28 days, then the patient can be transferred to the oral form of the drug at a dose of 0.3-0.6 g per day.
Pills
According to the instructions, Tiolepta in the form of tablets is taken orally, without chewing, on an empty stomach, about half an hour before the first meal, with water (sufficient amount).
The daily dose is 2 tablets of 300 mg each or 1 tablet of Tiolepta 600 mg. The maximum daily dose is 0.6 g.
The duration of therapy is determined by the doctor on an individual basis.
Side effects
Solution for infusion
- after intravenous administration: thrombophlebitis, hemorrhagic rash (purpura), thrombocytopenia, punctate hemorrhages in the skin or mucous membranes, diplopia, convulsions;
- with rapid introduction: difficulty breathing, increased intracranial pressure (the appearance of a feeling of heaviness in the head);
- allergic reactions: systemic allergic reactions (up to the development of anaphylactic shock), urticaria;
- hypoglycemia (due to improved absorption of glucose).
Pills
Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare):
- immune system: very rarely - systemic allergic reactions (up to the development of anaphylactic shock);
- nervous system: very rarely - a violation or change in taste;
- gastrointestinal tract: very rarely - diarrhea, abdominal pain, vomiting, nausea;
- skin and subcutaneous tissue: very rarely - allergic reactions in the form of rash, eczema, itching, urticaria;
- metabolism: very rarely - a decrease in the concentration of glucose in the blood is possible due to an improvement in the absorption of glucose, which may manifest itself as symptoms of hypoglycemia (visual impairment, headache, increased sweating, dizziness).
Overdose
The main symptoms of an overdose when taking Thiolepta inside: vomiting, nausea, headache.
Therapy is symptomatic (including gastric lavage, the appointment of activated carbon). If necessary, anticonvulsant treatment is carried out and measures are taken to maintain vital body functions.
special instructions
During the period of therapy for diabetes mellitus, constant monitoring of the concentration of glucose in the blood is required, especially at the beginning of the use of the drug. In order to avoid the development of hypoglycemia, in some cases, the dose of insulin or an oral hypoglycemic agent is reduced.
Alcohol should not be consumed during treatment.
Influence on the ability to drive vehicles and complex mechanisms
During the period of application of the solution for infusion, care should be taken when driving vehicles and conducting potentially hazardous activities.
Application during pregnancy and lactation
The experience of using Tiolepta during pregnancy and lactation is not sufficient, and therefore the drug is contraindicated during gestation and during breastfeeding.
Pediatric use
Due to the fact that the safety and efficacy of using the drug in children and adolescents under the age of 18 have not been established, Thiolepta is contraindicated in patients of this age category.
Drug interactions
The effect of thioctic acid on drugs / substances in combination therapy:
- cisplatin: reduces its effectiveness;
- insulin, oral hypoglycemic agents: may enhance their effect;
- glucocorticosteroids: enhances their anti-inflammatory effect.
The action of thioctic acid is weakened by ethanol and its metabolites.
Due to the fact that thioctic acid binds metals, it should not be used in combination with drugs that contain metals (for example, calcium, magnesium, iron preparations), as well as with dairy products (since they contain calcium) … If such a combination is necessary, an interval between doses of at least 2 hours should be observed.
Analogs
The analogues of Thiolepta are: Espa-Lipon, Thiolipon, Thioctic acid, Thioctacid BV, Thiogamma, Polytion, Octolipen, Neurolipon, Lipothioxon, Lipoic acid, Berlition 300.
Terms and conditions of storage
Store in a place protected from light and moisture at temperatures up to 25 ° C. Keep out of the reach of children.
Shelf life: solution - 3 years; tablets - 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tiolept
According to reviews, Tiolepta in tablets is an effective drug when used in complex therapy, which practically does not cause side effects and does not affect driving. It is also noted that the drug helps only with a course admission, in addition, the individual characteristics of patients significantly affect its effectiveness.
Among the disadvantages, the high cost of the drug is noted.
Price for Tiolepta in pharmacies
The approximate price of Tiolepta in the form of a solution for infusion (50 ml per package) is 150 rubles; Tiolepta tablets 600 mg (60 pcs. in a package) - 833 rubles.
Tiolepta: prices in online pharmacies
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Drug name Price Pharmacy |
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Tiolepta 300 mg film-coated tablets 30 pcs. 148 RUB Buy |
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Tiolepta 12 mg / ml solution for infusion 50 ml 1 pc. 184 r Buy |
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Thiolepta tablets p.p. 300mg 30 pcs. 255 RUB Buy |
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Tiolepta 600 mg film-coated tablets 30 pcs. 359 r Buy |
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Thiolepta tablets p.p. 600mg 30 pcs. RUB 580 Buy |
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Tiolepta 600 mg film-coated tablets 60 pcs. 751 RUB Buy |
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Thiolepta tablets p.p. 600mg 60 pcs. 901 RUB Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
