Description
Release form
Concentrate for solution for infusion.
Packaging
5 ampoules
Pharmacological action
Pharmacodynamics
Thioctic ( -lipoic) acid – an endogenous antioxidant (binds free radicals), is formed in the body during oxidative decarboxylation of -keto acids. As a coenzyme of mitochondrial multienzyme complexes, it participates in the oxidative carboxylation of pyruvic acid and β-keto acids.
Helps lower blood glucose and increase glycogen in the liver, as well as overcome insulin resistance. The nature of the biochemical action is close to the B vitamins. Participates in the regulation of lipid and carbohydrate metabolism, stimulates cholesterol metabolism, improves liver function.
Has hepatoprotective, hypolipidemic, hypocholesterolemic, hypoglycemic effect.
The use of ethylenediamine salt of thioctic acid in solutions for iv administration (having a neutral reaction) can reduce the severity of adverse reactions.
Pharmacokinetics
Absorption and distribution of
With the on / in the introduction of Cmax is 25-38 μg / ml and is achieved after 10-11 minutes, AUC – about 5 μg x h / ml.
Vd – about 450 ml / kg.
Metabolism and excretion
Has the effect of first passing through the liver. The formation of metabolites occurs as a result of side chain oxidation and conjugation. Thioctic acid and its metabolites are excreted in the urine (80-90%).
Indications
Diabetic polyneuropathy. Alcoholic polyneuropathy.
Contraindications
Hypersensitivity to the components of the drug
children’s age (efficacy and safety not established)
pregnancy (lack of sufficient experience with the drug)
breastfeeding (lack of sufficient experience with the drug).
Use during pregnancy and lactation
Contraindicated in pregnancy. At the time of treatment, breastfeeding should be stopped (there is not enough experience with these cases).
Special instructions
Recent clinical studies have shown that thioctic (a-lipoic) acid is highly effective in patients with type 2 diabetes with cardiovascular manifestations of diabetic neuropathy. The therapeutic effect of Berlition in this group of patients may be the result of the effect of the drug on the autonomic nervous system, in particular by increasing the speed of wave propagation in visceral parasympathetic and sympathetic fibers.
Use in pediatrics
Berlition can not be prescribed for children and adolescents due to the lack of clinical experience with the drug in this category of patients.
Composition
1 ml (1 ampoule) contains:
Active ingredient:
ethylenediamine salt of thioctic (? -lipoic) acid 64.66 mg (776 mg), which corresponds to a content of thioctic (? -lipoic) acid 50 mg (600 mg).
Excipients:
propylene glycol,
ethylenediamine,
d / i water.
Dosage and administration of
In severe forms of polyneuropathy at the beginning of treatment, the drug is prescribed iv 300-600 mg (12-24 ml, respectively) / day for 2-4 weeks. In the future, they switch to maintenance therapy and prescribe 300 mg tablets (1 tab.) 1 time / day.
When i / m is administered, the dose administered at one injection site should not exceed 50 mg (2 ml). Intramuscular administration of the drug in high doses must be carried out in the form of several injections (2 ml per injection site).
Side effects of the
From the side of the central nervous system: very rarely – cramps, diplopia with rapid on / on administration, feelings of heaviness in the head (increased intracranial pressure) and breathing difficulties that pass on their own are possible.
From the blood coagulation system: very rarely – petechiae on the skin and mucous membranes, thrombocytopathy, hemorrhagic rash (purpura), thrombophlebitis.
On the part of the metabolism: possibly hypoglycemia (due to improved glucose uptake).
Allergic reactions: possibly urticaria, systemic allergic reactions up to anaphylactic shock.
Local reactions: possibly – burning at the injection site.
Drug Interactions
In vitro thioctic (a-lipoic) acid reacts with complexes containing metal ions (for example, cisplatin). Therefore, while taking cisplatin, weakening of the action of Berlition is possible.
With the simultaneous use of ethanol and its metabolites can lead to a weakening effect of Berlition.
Berlition enhances the hypoglycemic effect of insulin and oral hypoglycemic agents.
Pharmaceutical interaction
Thioctic (a-lipoic) acid forms sparingly soluble complex compounds with glucose molecules (including levulose solutions).
Berlition is incompatible with glucose solutions, Ringer’s solution, as well as with solutions that are known to react with SH-groups or disulfide bridges.
Overdose
Symptoms: nausea, vomiting, headache.
In severe cases: psychomotor excitation or turbidity of consciousness, generalized convulsions, severe disorders of acid-base balance, lactic acidosis, hypoglycemia (up to the development of coma), acute skeletal muscle necrosis, DIC-syngod syndrome.
Treatment: With suspected thioctic acid intoxication (e.g. the introduction of more than 80 mg of thioctic acid per 1 kg of body weight) emergency hospitalization and immediate application of measures in accordance with the general principles adopted in the case of accidental poisoning is recommended. Therapy is symptomatic. Treatment of generalized seizures, lactic acidosis and other life-threatening effects of intoxication should be carried out in accordance with the principles of modern intensive care. There is no specific antidote. Hemodialysis, hemoperfusion or filtration methods with forced removal of thioctic acid are not effective.
Storage Conditions
Store in a cool, dry, dark place.
Shelf life
3 years.
Deystvuyushtee substance
Tioktovaya Chisloth
drugstore
drugstore
Dosage form
infusion solution
Possible product names
BERLITION 600 0.025 / ML 24ML N5 AMP CONCER D / R-RA
25 BERLIT. 24ML. No. 5 END. D / INF. AMP. / BERLIN-CHEMIS /
Berlition 600 ampoules 600 mg, 24 ml, 5 pcs.
Berlition 600 U solution d / injection. 25 mg / ml 24 ml No. 5 amp.
Berlition 600 conc d / r d / inf 25mg / ml 24ml N5 amp t / s
