Dialipon (solution)

General characteristics. Structure:

Active ingredient: thioctic acid;

1 ml of solution contains meglyuminovy salt of alpha lipoic acid 58,382 mg that corresponds to 30 mg of alpha lipoic acid in terms of 100% substance;

excipients: N-metilglyukamin (Megluminum), polyethyleneglycol 300 (a macrogoal 300), water for injections.

Pharmacological properties:

Pharmacodynamics. α-lipoic acid acid acts as coenzyme in oxidizing decarboxylation of α-ketonic acids;;;;;;;;;; plays an important role in energy balance of a cell. In an amide form (липоамид) is an essential cofactor of the multienzymatic complexes catalyzing decarboxylation of α-ketonic acids of a tricarbonic acid cycle. acid anti-toxic and antioxidant properties are inherent in α-lipoic acid, it is also capable to recover other antioxidants, in particular, at a diabetes mellitus. At patients with diabetes α-lipoic acid acid reduces resistance to insulin and slows down development of peripheral neuropathy. Promotes decrease in content of glucose in blood and to accumulation of a glycogen in a liver. α-lipoic acid acid influences cholesterol exchange, takes part in regulation of lipidic and carbohydrate metabolism, improves function of a liver (owing to hepatoprotective, antioxidant, disintoxication action). Also α-lipoic acid acid well influences regeneration processes.

Pharmacokinetics. Elimination half-life of drug of 30 minutes. The general clearance makes 694 ml/minute. Distribution volume – 12,7 l. After one-time intravenous administration in the first 3-6 hours with urine 93-97% of α-lipoic acid of acid or its derivatives are removed.

Pharmaceutical characteristics

 

Main physical and chemical properties: transparent yellow liquid.

Incompatibility. Dialipon reacts in vitro with ionic complexes of metals (for example, with Cisplatinum) therefore drug can reduce their effect. Dialipon with sugars forms difficult soluble complex compounds. Because of it infusion solution of Dialipon is incompatible with solutions of glucose, fructose, Ringera. Drug is incompatible with the solutions containing connections which react with SH groups or disulfide bridges.

Indications to use:

As a part of complex therapy of polineyropatiya of various genesis (diabetic polyneuropathy, alcoholic polyneuropathy), at atherosclerosis (as hypolipidemic means), liver diseases (hepatitises, cirrhosis, fatty dystrophy of a liver in the absence of hepatitis B), at acute and chronic intoxications (poisonings with salts of heavy metals, mushrooms).

Route of administration and doses:

Drug is appointed for intravenous injections / infusions after preliminary cultivation in 0,9% chloride sodium solution.

At heavy diabetic polyneuropathy treatment of adults begin with infusion 20 ml of the solution (600 mg α-lipoic acid) divorced in 250 ml of 0,9% of solution of sodium of chloride, 1 time a day. Enter slowly – no more than 50 mg of α-lipoic acid of acid (1,7 ml of solution for infusions) in a minute. In very hard cases the daily dose is increased to 900 - 1200 mg/days.

The initial course of treatment is conducted for 2-4 weeks. Afterwards pass to a maintenance therapy with dosage forms of α-lipoic acid of acid for oral administration (Dialipon capsules) in a dose of 600 mg of drug 1–3 times a day for 1 - 3 months.

For prevention of diabetic polyneuropathy, at atherosclerosis, chronic intoxications, liver diseases the dose of drug is established individually, depending on age, by body weights of the patient and severity of a disease. It is necessary to begin treatment with an initial dose of 10 ml of solution (300 mg of α-lipoic acid of acid) in days.

The course of therapy by Dialipon is recommended to carry out 2 times a year.

Features of use:

Use during pregnancy or feeding by a breast

 

Drug Dialipon is contraindicated to use at pregnancy. In need of its use during a lactation it is necessary to stop feeding by a breast. In pilot studies on animals teratogenic effect of thioctic acid was not revealed. Similar researches at people were not conducted. There are no data on release of thioctic acid in breast milk.

Children

 

Dialipon cannot appoint children and teenagers due to the lack of clinical experience of use of drug for this category of patients.

 

At treatment of patients with a diabetes mellitus frequent control of a glycemia is necessary. In certain cases it is necessary to skorregirovat doses of antihyperglycemic means for the prevention of a hypoglycemia.

During treatment of polyneuropathy, thanks to regeneration processes, perhaps short-term strengthening of sensitivity which is followed by paresthesia with feeling of "crawling of goosebumps".

Constant alcohol intake is risk factor of development of polyneuropathy and can reduce Dialipon's efficiency. Therefore it is recommended to refrain from alcohol intake during treatment by drug. It is not necessary to appoint Dialipon along with the drugs containing metals (iron preparations, magnesium, calcium).

Drug is light-sensitive therefore ampoules should be got from packaging only just before use.

Infusion solutions should be protected from a sunlight, covering them with light-protective packages. In these conditions the prepared infusion solution remains is suitable no more than 6 hours.

Ability to influence speed of response at control of motor transport or work with other mechanisms

 

Drug does not influence speed of response at control of motor transport or work with other mechanisms, but in case of signs of side effect of drug (see. "Side reactions") it is necessary to refrain from this occupation.

Side effects:

At a bystry intravenous injection heavy feelings in the head, increase in intracranial pressure, hot inflows, perspiration, nausea, vomiting, a short-term delay or difficulty of breath which take place independently are possible.

From a nervous system: in certain cases after intravenous administration the headache, dizziness, spasms, a diplopia, vision disorders were observed.

From system of a hemopoiesis: in certain cases after intravenous administration petekhialny hemorrhages in mucous membranes, skin, a trombotsitopatiya, dysfunction of thrombocytes, hypocoagulation, hemorrhagic rash (purpura), thrombophlebitis were observed.

From a metabolism: a hypoglycemia (dizziness, the raised potovydeleniye, a headache, a visual disturbance) owing to glucose utilization improvement.

Allergic reactions: at intravenous administration in an injection site emergence of a small tortoiseshell and development of eczema, petekhialny rashes, an itch, dermatitis is possible; seldom - system allergic reactions up to an acute anaphylaxis.

Local reactions: sometimes – at patients with hypersensitivity in the place of an injection of Dialipon the feeling of a thermalgia is possible.

Disturbances from cardiovascular system: pain in heart, tachycardia.

Interaction with other medicines:

Strengthening of hypoglycemic effect at reception of insulin or peroral antihyperglycemic means therefore constant control of level of a glycemia, especially in an initiation of treatment Dialipon and correction of doses of hypoglycemic means is necessary is possible. Simultaneous use can bring to loss of activity of Cisplatinum.

Contraindications:

Hypersensitivity to drug or to one of its components; children's age; period of pregnancy and feeding by a breast.

Overdose:

At overdose nausea, vomiting, a headache are possible. At overdose or suspicion on development of serious side effects it is necessary to stop immediately an injection and, without taking out a syringe needle, to carry out through it slow injection of 0,9% of solution of sodium of chloride.

There are data that owing to accidental or intended use of lipoic acid in a dose of 10-40 g against the background of a drunkenness isolated cases with serious priznaky intoxications were observed up to a fatal outcome. Clinical signs of intoxication were shown in the form of psychomotor disturbance or a faint with the subsequent generalized spasms and development of a lactacidemia. Lipoic acid the hypoglycemia, shock, рабдомиолиз, hemolysis, the disseminated intravascular coagulation, oppression of marrow and organ insufficiency are a consequence of intoxication.

At acute poisoning with lipoic acid immediate hospitalization with holding all-therapeutic actions of a detoxication of an organism is shown (an artificial respiration, vomiting, a gastric lavage, absorbent carbon, etc.). For treatment of generalized spasms, a lactacidemia and other effects of intoxication it is necessary to be guided by means of a modern intensive care and symptomatic approach for acceleration of removal of lipoic acid. Symptomatic further treatment.

Storage conditions:

Period of validity. 5 years. Not to use drug after the termination of the period of validity specified on packaging. To store in the place protected from light at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

On 10 ml or 20 ml in an ampoule, on 5 or 10 ampoules in a pack.