Thiolipon 600 mg 30 pcs. film-coated tablets
pharmachologic effect
Thioctic acid (alpha-lipoic acid) is an endogenous antioxidant (binds free radicals), formed in the body during the oxidative decarboxylation of alpha-keto acids. As a coenzyme of mitochondrial multienzyme complexes, it participates in the oxidative decarboxylation of pyruvic acid and alpha-keto acids. Helps reduce blood glucose concentrations and increase glycogen in the liver, as well as overcome insulin resistance. By the nature of its biochemical action it is close to B vitamins. Participates in the regulation of lipid and carbohydrate metabolism, stimulates cholesterol metabolism, and improves liver function. It has hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effects. Improves trophism of neurons.
Composition and release form Thiolipon 600 mg 30 pcs. film-coated tablets
Tablet - 1 tablet:
- Active substance: thioctic acid (lipoic acid) - 600 mg;
- Core excipients: colloidal silicon dioxide (Aerosil) - 12.3 mg, microcrystalline cellulose - 41 mg, hypromellose (hydroxypropyl methylcellulose) - 8.2 mg, sodium carboxymethyl starch (Primogel) - 28.7 mg, magnesium stearate - 8.2 mg , calcium stearate monohydrate - 8.2 mg, sodium stearyl fumarate - 8.2 mg, magnesium hydroxylicate (talc) - 24.6 mg, lactose monohydrate (milk sugar) - 80.6 mg.
30 pcs. packaged.
Description of the dosage form
Oblong tablets with a score on one side. On a cross section, two layers are visible: the outer one is yellow or yellow with a greenish tint, the inner one is light yellow.
Directions for use and doses
Prescribed orally 600 mg once a day.
The minimum course of therapy is 3 months. In some cases, taking the drug requires longer treatment, the duration of which is determined by the doctor.
The tablets are taken on an empty stomach, approximately 30 minutes before the first meal, without chewing and with a small amount of water.
Pharmacokinetics
When taken orally, it is quickly and completely absorbed from the gastrointestinal tract (taken with food reduces absorption). The time to reach maximum concentration is 40 - 60 minutes. Bioavailability - 30%.
Has a “first pass” effect through the liver. The formation of metabolites occurs as a result of side chain oxidation and conjugation.
Volume of distribution is about 450 ml/kg. Thioctic acid and its metabolites are excreted by the kidneys (80 - 90%). The half-life is 20 - 50 minutes. Total plasma clearance is 10 - 15 ml/min.
Indications for use Thiolipon 600 mg 30 pcs. film-coated tablets
Diabetic polyneuropathy; alcoholic polyneuropathy.
Contraindications
- Hypersensitivity to Thiolipon components;
- pregnancy, breastfeeding period (there is no sufficient experience in using the drug);
- children under 18 years of age (efficacy and safety of use have not been established);
- lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Application Thiolipon 600 mg 30 pcs. film-coated tablets during pregnancy and breastfeeding
Contraindicated during pregnancy. During treatment, breastfeeding should be stopped (there is not enough experience in these cases).
Children under 18 years of age.
special instructions
Patients taking Thiolipon should avoid drinking alcohol.
In patients with diabetes mellitus, constant monitoring of blood glucose concentration is necessary, especially at the initial stage of therapy. In some cases, it is necessary to reduce the dose of insulin or oral hypoglycemic drug to avoid the development of hypoglycemia.
During hypoglycemia, the ability to concentrate and react quickly to drive a car or operate machinery may be impaired.
Impact on the ability to drive vehicles and machinery.
The drug does not affect the ability to drive vehicles or operate machinery that requires increased attention.
Side effects Thiolipon 600 mg 30 pcs. film-coated tablets
Possible dyspepsia, including nausea, vomiting, heartburn.
In some cases, the development of allergic skin reactions (urticaria) is possible.
Anaphylactic shock.
Hypoglycemia may develop (due to improved glucose absorption).
Drug interactions
Thioctic acid reacts with ionic metal complexes (for example, with cisplatin), therefore, with simultaneous use of the drug Thiolipon, the effect of cisplatin may be reduced. After taking Thiolipon in the morning, it is recommended to take iron and magnesium supplements, and also consume dairy products (due to their calcium content) in the afternoon or evening.
When used simultaneously, thioctic acid enhances the effect of insulin and oral hypoglycemic agents.
Alcohol (ethanol) reduces the therapeutic activity of thioctic acid.
Thiolipon
Thiolipon tablet film 600 mg x30 ATX code: A16AX01 (Thioctic acid) Active substance: thioctic acid BAN accepted for use in the UK
Dosage form
Thiolipon
Tab., cover. film-coated, 600 mg: 20, 30, 40 or 50 pcs.reg. No.: LP-001209 dated 11/15/11 - Valid
Release form, packaging and composition
Film-coated tablets 1 tab.
thioctic acid 600 mg Clinical-pharmacological group: Drug regulating lipid and carbohydrate metabolism Pharmaco-therapeutic group: Metabolic agent
Pharmacological action The drug is an endogenous antioxidant that binds free radicals. Thioctic (α-lipoic) acid is involved in the mitochondrial metabolism of the cell; it functions as a coenzyme in the complex for the transformation of substances that have a pronounced antitoxic effect. They protect the cell from reactive radicals arising during intermediate metabolism or during the breakdown of exogenous foreign substances, and from heavy metals. Thioctic acid exhibits synergism with insulin, which is associated with increased glucose utilization. In patients with diabetes mellitus, thioctic acid leads to a change in the concentration of pyruvic acid in the blood.
Indications for the drug: Diabetic polyneuropathy. ICD-10 codes
ICD-10 code Indication
G63.2 Diabetic polyneuropathy
Dosage regimen The method of administration and dosage regimen of a particular drug depend on its release form and other factors. The optimal dosage regimen is determined by the doctor. The compliance of the dosage form of a particular drug with the indications for use and dosage regimen should be strictly observed.
When taken orally, a single dose is 600 mg.
300-600 mg/day is administered intravenously (slow stream or drip).
Side effect
After intravenous administration, diplopia, convulsions, pinpoint hemorrhages in the mucous membranes and skin, impaired platelet function are possible; with rapid administration, an increase in intracranial pressure.
When taken orally, dyspeptic symptoms are possible (including nausea, vomiting, heartburn).
When taken orally or intravenously - allergic reactions (urticaria, anaphylactic shock), hypoglycemia.
Contraindications for use: Pregnancy, lactation (breastfeeding), hypersensitivity to thioctic acid.
special instructions
With simultaneous use, it is possible to enhance the hypoglycemic effect of insulin and oral hypoglycemic agents.
When used simultaneously with cisplatin, its effectiveness may be reduced.
Thiolipon tablets PPO 600 mg No. 30
Compound
Active substance: thioctic acid - 600 mg.
Pharmacokinetics
When taken orally, it is quickly and completely absorbed from the gastrointestinal tract. Cmax is reached 30 minutes after administration and is 4 mcg/ml.
With intravenous administration of thioctic acid at a dose of 600 mg, Cmax in blood plasma after 30 minutes is about 20 mcg/ml.
Thioctic acid has a “first pass” effect through the liver. The formation of metabolites occurs as a result of side chain oxidation and conjugation. Vd - about 450 ml/kg.
Thioctic acid and its metabolites are excreted by the kidneys mainly in the form of metabolites (80-90%), in small quantities - unchanged. T1/2 is 25 min. Total plasma clearance is 10-15 ml/min/kg.
Indications for use
- Diabetic polyneuropathy.
- Alcoholic polyneuropathy.
Contraindications
- Hypersensitivity to thioctic acid or any of the excipients of the drug.
- Pregnancy, breastfeeding period.
- Children under 18 years of age (efficacy and safety of use have not been established).
- Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.
Directions for use and doses
Prescribed orally 600 mg once a day. The tablets are taken on an empty stomach, approximately 30 minutes before the first meal (breakfast), without chewing and with a sufficient amount of water.
The maximum daily dose is 600 mg.
The minimum course of therapy is 3 months.
In some cases, taking the drug involves longer use, the timing of which is determined by the attending physician.
Storage conditions
In a place protected from light, at a temperature not exceeding 25°C.
Keep out of the reach of children.
Best before date
3 years. Do not use after the expiration date.
special instructions
Alcohol intake reduces the effectiveness of thioctic acid, so patients during therapy should refrain from drinking alcohol throughout the entire course of treatment, and also, if possible, in between courses. Alcohol consumption during thioctic acid therapy is also a risk factor for the development and progression of neuropathy.
In patients with diabetes mellitus, constant monitoring of blood glucose concentrations is necessary, especially at the initial stage of therapy. In some cases, it is necessary to reduce the dose of insulin or oral hypoglycemic drug to avoid the development of hypoglycemia.
Concomitant food intake may interfere with the absorption of thioctic acid.
When taking the drug, it is not recommended to consume dairy products (due to the calcium content in them). The interval between taking thioctic acid and consuming dairy products should be at least 2 hours.
Several cases of the development of AIS have been reported in patients with diabetes mellitus during therapy with thioctic acid, which was characterized by frequent hypoglycemia in the presence of autoantibodies to insulin. The possibility of developing AIS is determined by the presence in patients with a certain HLA (human leukocyte antigen) genotype of the HLA-DRB 1*04:06 and HLA-DRB 1*04:03 alleles.
In severe cases, treatment begins with parenteral use of thioctic acid (intravenous administration) for 2-4 weeks, then the patient is transferred to oral administration of thioctic acid.
The possibility of autoimmune insulin syndrome should be considered in the differential diagnosis of spontaneous hypoglycemia in patients taking thioctic acid.
Description
Metabolic agent.
Dosage form
Oblong film-coated tablets with a score line on one side.
On a cross section, two layers are visible: the outer one is yellow or yellow with a greenish tint, the inner one is light yellow.
Use in children
Contraindicated for use in children and adolescents under 18 years of age.
Pharmacodynamics
It is an endogenous antioxidant that binds free radicals. Thioctic (α-lipoic) acid is involved in the mitochondrial metabolism of the cell; it functions as a coenzyme in the complex for the transformation of substances that have a pronounced antitoxic effect. They protect the cell from reactive radicals arising during intermediate metabolism or during the breakdown of exogenous foreign substances, and from heavy metals. Thioctic acid exhibits synergism with insulin, which is associated with increased glucose utilization. In patients with diabetes mellitus, thioctic acid leads to a change in the concentration of pyruvic acid in the blood.
Side effects
From the immune system: very rarely - allergic reactions (skin rash, eczema, urticaria, itching); frequency unknown - anaphylactic shock, autoimmune insulin syndrome in patients with diabetes mellitus, which is characterized by frequent hypoglycemia in the presence of autoantibodies to insulin.
On the metabolic side: very rarely - hypoglycemia (due to improved absorption of glucose), symptoms of which include dizziness, increased sweating, headache and blurred vision.
From the nervous system: often - dizziness; very rarely - changes or disturbances in taste sensations, hot flashes, convulsions.
From the digestive system: often - nausea, vomiting; very rarely - abdominal pain, diarrhea.
From the hematopoietic system: after intravenous administration, very rarely - petechial hemorrhages in the mucous membranes, skin; hemorrhagic rash (purpura), thrombocytopathy, hypocoagulation.
From the liver and biliary tract: after intravenous administration, very rarely - increased activity of liver enzymes.
From the cardiovascular system: with rapid intravenous administration, very rarely - thrombophlebitis, pain in the heart, tachycardia.
On the part of the organ of vision: after intravenous administration, very rarely - diplopia, blurred vision.
Local reactions: after intravenous administration, very rarely - a burning sensation at the injection site, frequency unknown - allergic reactions at the injection site (irritation, hyperemia or swelling).
Other: with rapid intravenous administration, very rarely - self-limiting increase in intracranial pressure (feeling of heaviness in the head) and difficulty breathing, weakness.
Use during pregnancy and breastfeeding
Contraindicated for use during pregnancy and lactation (breastfeeding). If it is necessary to use it during lactation, the issue of stopping breastfeeding should be decided.
Interaction
With simultaneous use of thioctic acid and cisplatin, a decrease in the effectiveness of cisplatin is observed.
Thioctic acid is capable of forming chelate complexes with metals; co-administration with iron, magnesium, and calcium preparations should be avoided. Keep in mind that dairy products contain calcium. Therefore, it is also necessary to avoid using thioctic acid simultaneously with dairy products (due to their calcium content).
With simultaneous use of thioctic acid and insulin or oral hypoglycemic drugs, their effect may be enhanced, therefore regular monitoring of blood glucose levels is recommended, especially at the beginning of therapy with thioctic acid. In some cases, it is permissible to reduce the dose of hypoglycemic drugs to avoid the development of symptoms of hypoglycemia.
Thioctic acid enhances the anti-inflammatory effect of GCS.
Ethanol and its metabolites weaken the effect of thioctic acid.
Thioctic acid forms poorly soluble complex compounds with sugar molecules. Thioctic acid is incompatible with solutions of dextrose (glucose), fructose, Ringer, as well as with solutions that react with disulfide or SH groups.
Overdose
Symptoms: headache, nausea, vomiting.
In the case of an acute overdose of thioctic acid (when using 10-40 g), serious signs of intoxication may be observed (generalized convulsive attacks; severe acid-base imbalance leading to lactic acidosis; hypoglycemic coma; severe blood clotting disorders, sometimes leading to death).
If a significant overdose of the drug is suspected (doses equivalent to more than 10 tablets for an adult or more than 50 mg/kg body weight for a child), immediate hospitalization is necessary.
Treatment: symptomatic (including gastric lavage, taking activated charcoal), if necessary - anticonvulsant therapy, measures to maintain vital body functions. There is no specific antidote. Hemodialysis is ineffective.
Impact on the ability to drive vehicles and operate machinery
During the period of use of thioctic acid, patients should be careful when driving vehicles and machinery, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.
