Thiolipon
Tiolipon: 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: Thiolipon
ATX code: A16AX01
Active ingredient: Thioctic acid (Thioctic acid)
Manufacturer: Biosynthesis, JSC (Russia)
Description and photo update: 2018-24-10
Prices in pharmacies: from 370 rubles.
Buy
Thiolipon is a drug used in the treatment of diabetic / alcoholic polyneuropathy.
Release form and composition
Dosage forms of Thiolipon:
- film-coated tablets: shell - yellow or yellow with a greenish tinge, core - light yellow; 300 mg each - round, biconvex; 600 mg each - oblong, on one side with a line (in a cardboard box 1 dark glass jar, in a jar of 30 or 50 tablets; in a cardboard box 1-3 blisters, 10 pcs in a package);
- concentrate for the preparation of a solution for intravenous administration: transparent, greenish-yellow (in a cardboard box 10 ampoules or 1-2 packs of 5 ampoules).
Composition of 1 tablet Tiolipon:
- active substance: thioctic acid (lipoic acid) - 300 or 600 mg;
- auxiliary components (300/600 mg): calcium stearate monohydrate - 5 / 8.2 mg; lactose monohydrate (milk sugar) - 91.5 / 80.6 mg; sodium stearyl fumarate - 5 / 8.2 mg; hypromellose - 5 / 8.2 mg; sodium carboxymethyl starch (primogel) - 17.5 / 28.7 mg; colloidal silicon dioxide - 7.5 / 12.3 mg; microcrystalline cellulose - 50/41 mg; magnesium stearate - 5 / 8.2 mg; magnesium hydrosilicate - 13.5 / 24.6 mg;
- shell (300/600 mg): Opadry II (hypromellose - 3.4 / 4.1 mg; macrogol 4000 -1.1 / 1.3 mg; lactose monohydrate - 3 / 3.6 mg) - 10/12 mg; coloring pigments - 2.5 / 3 mg; titanium dioxide (E 171) - 2 / 2.4 mg; aluminum varnish based on quinoline yellow (E 104) - 0.4 / 0.48 mg; aluminum varnish based on indigo carmine (E 132) - 0.05 / 0.06 mg; aluminum varnish based on sunset yellow (E 110) - 0.05 / 0.06 mg.
Composition of 1 ml of Tiolipon concentrate:
- active substance: thioctic acid (lipoic acid) - 30 mg;
- auxiliary components: propylene glycol, ethylenediamine, water for injection.
Pharmacological properties
Pharmacodynamics
Thioctic acid (alpha-lipoic acid) is an endogenous antioxidant (binds free radicals), formed in the body during the oxidative decarboxylation of alpha-keto acids.
It has hypolipidemic, hepatoprotective, hypoglycemic and hypocholesterolemic effects.
As a coenzyme of mitochondrial multienzyme complexes, it takes part in the oxidative decarboxylation of alpha-keto acids and pyruvic acid. Promotes an increase in glycogen in the liver and a decrease in the concentration of glucose in the blood, as well as overcoming insulin resistance.
By the nature of its biochemical action, lipoic acid is close to vitamins of group B. It is necessary for carbohydrate and lipid metabolism, stimulates cholesterol metabolism, improves liver function and neuronal trophism.
Pharmacokinetics
- intravenous administration: C max (maximum concentration) is 0.025–0.038 mg / ml, the time to reach it is 10–11 minutes, the area under the concentration-time curve is approximately 0.005 mg / ml;
- oral administration: lipoic acid is completely and rapidly absorbed from the gastrointestinal tract, while absorption decreases when the drug is taken simultaneously with food. The time to reach maximum concentration is 40 to 60 minutes.
Bioavailability is 30%. Lipoic acid has a "first pass" effect through the liver. As a result of side chain oxidation and conjugation, metabolites are formed.
The volume of distribution is approximately 450 ml / kg. Thioctic acid and its metabolites are excreted by the kidneys (80–90%). The half-life is 20-50 minutes. The total plasma clearance is 10-15 ml / min.
Indications for use
Thiolipon is prescribed for the treatment of diabetic / alcoholic polyneuropathy.
Contraindications
Absolute:
- lactase deficiency, lactose intolerance, glucose-galactose malabsorption (tablets);
- pregnancy and the period of breastfeeding;
- age up to 18 years;
- individual intolerance to any component of the drug.
Relative (Tiolipon is prescribed under medical supervision):
- diabetes mellitus (tablets);
- chronic alcoholism (pills).
Instructions for the use of Tiolipon: method and dosage
Pills
Thiolipon is taken orally with a small amount of water, without chewing.
The tablets are taken once a day on an empty stomach, about 30 minutes before the first meal.
The daily dose is 600 mg.
The minimum course duration is 3 months (in some cases, longer therapy may be required).
Injection solution
Thiolipon is given intravenously. The concentrate must first be diluted in isotonic sodium chloride solution.
In severe forms of the disease, 300-600 mg is administered once a day as an intravenous drip infusion (for 50 minutes).
Duration of use is from 2 to 4 weeks. After the end of this period, the patient is transferred to oral administration of the drug (300–600 mg per day) for a course of at least 3 months.
Side effects
Possible side reactions: hypoglycemia (associated with improved glucose uptake), allergic reactions (including urticaria, anaphylactic shock).
Other possible violations:
- tablets: dyspepsia, including nausea, vomiting, heartburn;
- injection solution: very rarely - convulsions, diplopia, punctate hemorrhages in the skin and mucous membranes, thrombocytopathy, hemorrhagic rash, thrombophlebitis; with the rapid introduction of the solution - an increase in intracranial pressure (the appearance of a feeling of heaviness in the head), difficulty breathing (additional therapy is not required).
Overdose
Main symptoms: vomiting, nausea, headache.
There is no specific antidote. In case of an overdose, symptomatic therapy is performed.
special instructions
Patients with diabetes mellitus require constant monitoring of the concentration of glucose in the blood, especially in the initial stages of drug use. In some cases, the insulin / oral hypoglycemic drug dose may be lowered by your doctor to avoid hypoglycemia.
During the period of treatment, one should refrain from drinking alcohol, since this leads to a weakening of the therapeutic effect of thioctic acid.
Ampoules with a concentrate should be removed from the package immediately before use, which is associated with the photosensitivity of the active substance. During the infusion, it is advisable to protect the bottle with the solution from light (it is possible to use light-protective bags, aluminum foil). The maximum storage time of the prepared solution is 6 hours.
Influence on the ability to drive vehicles and complex mechanisms
Patients when driving vehicles should take into account the likelihood of developing hypoglycemia.
Application during pregnancy and lactation
According to the instructions, Tiolipon is not prescribed to women during pregnancy / lactation.
Pediatric use
Thiolipon is not prescribed for patients under the age of 18.
Drug interactions
Possible interactions:
- cisplatin: a decrease in its effectiveness (cisplatin is recommended to be taken after lunch or in the evening);
- magnesium / iron preparations, as well as dairy products due to the calcium they contain: since thioctic acid reacts with ionic metal complexes, the recommended time for using these drugs is after lunch or in the evening;
- alcohol (ethanol): a decrease in the therapeutic activity of Thiolipon;
- insulin and oral hypoglycemic agents: enhancement of their action.
Analogs
Thiolipon's analogs are: Berlition 300 or 600, Lipoic acid, Thiogamma, Polytion, Thioctic acid, Thiolepta, Thioctic acid-Vial, Neurolipon, Octolipen, Lipothioxon, Espa-Lipon.
Terms and conditions of storage
Store in a place protected from light at temperatures up to 25 ° C. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tiolipon
According to a few reviews, Tiolipon is an effective antioxidant drug. The development of side effects is rarely reported.
Price for Tiolipon in pharmacies
The approximate price for Tiolipon is:
- tablets (30 pcs. 600 mg each) - 944–990 rubles;
- concentrate (10 ampoules, 10 ml each) - 404 rubles.
Tiolipon: prices in online pharmacies
Drug name Price Pharmacy |
Thiolipon conc. for prig of solution for intravenous injection. 30mg / ml 10ml 10 pcs. 370 rbl. Buy |
Thiolipon 30 mg / ml concentrate for preparation of solution for intravenous administration 10 ml 10 pcs. 370 rbl. Buy |
Thiolipon tablets p.p. 300mg 30 pcs. 526 r Buy |
Tiolipon 300 mg film-coated tablets 30 pcs. 526 r 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!