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medicalmeds.eu Medicines Simple drugs of ascorbic acid (vitamin C). Ascorbic kislota-Darnitsa

Ascorbic kislota-Darnitsa

Препарат Аскорбиновая кислота-Дарница. ЗАО "Фармацевтическая фирма "Дарница" Украина



General characteristics. Structure:

Active ingredient: ascorbic acid;
1 ml of solution for injections contains 50 mg of ascorbic acid in terms of 100% substance;
excipients: Natrii hydrocarbonas, sodium metabisulphite (Е 223), dinatrium эдетат, water for injections.



Pharmacological properties:

Pharmacodynamics. Ascorbic acid, or vitamin C, concerns to group of water-soluble vitamins. Takes part in redoxreactions, takes part in many processes of exchange, in particular, in regulation of carbohydrate metabolism, exchange of aromatic amino acids, thyroxine, in synthesis of catecholamines, steroid hormones, insulin. Is a necessary component in the course of a blood coagulation, synthesis of collagen, procollagen, regeneration of connecting and bone fabrics. Regulates permeability of capillaries (oppresses hyaluronidase). Takes part in absorption of iron and synthesis of hemoglobin.

With participation of ascorbic acid there passes the inactivation of free radicals in this connection ascorbic acid prevents damage of membranes of cells, in particular, of lymphocytes from the damaging action of peroxide oxidation. Such action causes a number of immunomodulatory effects, in particular, strengthens a chemotaxis, synthesis and release of interferon, improves migration of lymphocytes.

Increases nonspecific and immune resistance of an organism.

In a human body it is not synthesized. Insufficient receipt with food leads to development hypo - or avitaminosis.

Pharmacokinetics. Communication with proteins of plasma – 25%. Concentration of ascorbic acid in a blood plasma normal makes about 10-20 mkg/ml, stocks in an organism – about 1,5 g. Time of achievement of the maximum concentration in a blood plasma at intramuscular introduction of Tmax – 15-20 minutes. Easily gets into leukocytes, thrombocytes, and then – into all fabrics; it is deposited in a back share of a hypophysis, bark of adrenal glands, an eye epithelium, interstitial cells of seminal glands, ovaries, a liver, a spleen, a pancreas, lungs, kidneys, an intestines wall, heart, muscles, a thyroid gland; gets through a placenta. Concentration of ascorbic acid in leukocytes and thrombocytes is higher, than in erythrocytes and in plasma. At scarce states concentration in leukocytes decreases later and more slowly and is considered as the best criterion for evaluation of deficit, than concentration in a blood plasma. It is metabolized preferential in a liver. It is removed by kidneys, intestines, пóтом, breast milk in the form of not changed ascorbate and metabolites. At high doses when concentration in plasma reaches more than 1,4 mg/dl, removal sharply amplifies, and the raised excretion remains after the reception termination. Smoking and alcohol intake accelerate destruction of ascorbic acid (transformation into inactive metabolites), sharply reducing its stocks in an organism.

Pharmaceutical characteristics.

Main physical and chemical properties: transparent colourless or slightly yellowish liquid.

Incompatibility.

Drug is incompatible with iron salts, oxidizers, salts of heavy metals, especially copper. There are messages that injections of ascorbic acid are incompatible with Aminophyllinum, Bleomycinum sulfate, erythromycin, naftsilliny sodium, sodium nitrofurantoin, the conjugated estrogen, sodium bicarbonate, diethanol amide of a sulfafurazol. Sometimes, depending on level рН or concentration, incompatibility with chloramphenicol is noted.


Indications to use:

–       Treatment of deficit of ascorbic acid, scurvy.

–       Bleedings (uterine, pulmonary, nasal, enteral, hepatic), hemorrhagic diathesis, bleedings as syndrome of a radial illness, capillary toxicosis; overdose of anticoagulants.

–       Fractures of bones, vyalogranuliruyushchy wounds.

–       Nephropathy of pregnant women, Addison's disease, addisonichesky crisis.

–       Various dystrophies, physical and intellectual overworks.

–       Pregnancy and period of feeding by a breast.

–       Various intoxications and infectious diseases.

–       As antioxidant as auxiliary therapy – at atherosclerosis, bronchial asthma, diffusion diseases of connecting fabric (a pseudorheumatism, a system lupus erythematosus, a scleroderma).


Route of administration and doses:

Ascorbic kislotu-Darnitsa appoint intramusculary and intravenously struyno or kapelno.
Intravenously struyno enter within 1-3 min. For intravenous drop administration a single dose dissolve 0,9% of solution of sodium of chloride in 50-100 ml and enter by slow intravenous infusion with a speed of 30-40 thaws a minute. Intramusculary enter deeply into a muscle. Doses establish individually, taking into account character and disease severity.
To adults and children 12 years usually are more senior appoint 50-150 mg a day (1-3 ml of 5% of solution). Duration of a course is caused by the nature of pathological process and efficiency of therapy (mono - or complex).
To children up to 12 years appoint intravenously in a daily dose 5-7 mg/kg of body weight in the form of 5% of solution (0,5-2 ml). Usually for children daily doses make:
aged up to 6 months – 30 mg;
aged from 6 up to 12 months – 35 mg;
age from 1 to 3 years – 40 mg;
aged from 4 up to 10 years – 45 mg;
aged from 11 up to 12 years – 50 mg.
The maximum daily dose for children up to 12 years – 100 mg.

Features of use:

In connection with a promoting effect of ascorbic acid on synthesis of corticosteroid hormones, it is necessary to monitor function of kidneys and arterial pressure.

At prolonged use of high doses oppression of function of the insulyarny device of a pancreas therefore in the course of its treatment it is regularly necessary to control is possible.

At patients with the increased content of iron in an organism it is necessary to apply ascorbic acid in the minimum doses.

Purpose of ascorbic acid to patients with quickly proliferating and intensively metastasizing tumors can activate process.

Ascorbic acid as reducer, can distort results of various laboratory tests (content in blood of glucose, bilirubin, activity of transaminases, LDG). With care use drug for treatment of patients with hypercoagulation, renal failures (a giperoksalaturiya, an urolithiasis in the anamnesis and others).

The patients who is on a diet with the low content of sodium should not appoint high doses of drug.

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

Influence of drug in the recommended doses on speed of response at control of motor transport or work with other mechanisms is improbable.


Side effects:

Ascorbic acid, as a rule, is well transferred, however development of side reactions is possible.
From the central and peripheral nervous system: a headache, feeling of fatigue, at prolonged use in high doses – a sleep disorder, increase in excitability of the central nervous system.
From digestive tract: stomach spasms, sometimes nausea, diarrhea.
From a metabolism: a hypervitaminosis With, at prolonged use in high doses – oppression of function of the insulyarny device of a pancreas (a hyperglycemia, a glucosuria) and synthesis of a glycogen, a delay of sodium and liquid, disturbance of exchange of zinc and copper.
From cardiovascular system: decrease in permeability of capillaries, deterioration in a trophicity of fabrics; at prolonged use in high doses – myocardium dystrophy, increase in arterial pressure, development of mikroangiopatiya.
From system of blood: at prolonged use in high doses – a thrombocytosis, a giperprotrombinemiya, thrombogeneses, an erythrocytopenia, a neutrophylic leukocytosis.
From an urinary system: the giperoksalaturiya is possible; at prolonged use in high doses – damage of the glomerular device of kidneys, formation of oxalic nephroliths.
Allergic reactions: very seldom – skin rashes, a dermahemia, an acute anaphylaxis.
Reactions in an injection site: at intravenous administration the feeling of heat is possible.
Another: at intravenous administration in high doses – threat of abortion.

Interaction with other medicines:

At simultaneous use with salicylates, streptocides of short action the risk of a crystalluria increases.

At simultaneous use of ascorbic acid with salicylates, ethinylestradiol, benzylpenicillin and tetracyclines concentration of these drugs in blood increases.

At simultaneous use with ascorbic acid of derivatives of coumarin and heparin, antibiotics efficiency of these drugs decreases.

High doses of ascorbic acid can reduce рН urine therefore the canalicular reabsorption of amphetamine and tricyclic antidepressants which are applied at the same time decreases.

At simultaneous use ascorbic acid reduces efficiency of oral contraceptives.

Tetracyclines and acetylsalicylic acid strengthen removal of ascorbic acid with urine.

At simultaneous use with barbiturates, a pyrimidine excretion of ascorbic acid with urine raises. Raises iron excretion at the patients accepting Deferoxaminum. Increases neutralization and the general clearance of alcohol. Increases removal of the drugs having alkali reaction (including alkaloids). In high doses raises renal excretion of a meksiletin.

The concomitant use of ascorbic acid and Deferoxaminum increases fabric toxicity of iron, especially in a cardiac muscle that can lead to a blood circulatory system decompensation. Vitamin C can be accepted only in 2 hours after Deferoxaminum injection. Long reception of high doses at persons who are treated by Disulfiramum slows down reaction Disulfiramum alcohol.

Reduces chronotropic action of an izoprenalin and therapeutic action of derivatives of a fenotiazin.


Contraindications:

Hypersensitivity to drug components. Hypercoagulation, thrombophlebitis, tendency to fibrinferments, diabetes mellitus, urolithiasis, in particular hyperoxaluria; a renal failure, hemochromatosis, a thalassemia, a polycythemia, leukemia, sideroblastny anemia, deficit glyukozo-6-fosfatdegidrogenazy, drepanocytic anemia, the progressing malignant diseases; Quincke's edema, small tortoiseshell.
Use during pregnancy or feeding by a breast.

The lack of vitamin C of a diet of pregnant women can be dangerous to a fruit, however its use in high doses can negatively affect fetation, there is also a threat of abortion. Therefore ascorbic acid is appointed only when the expected advantage for mother exceeds potential risk for a fruit. Ascorbic acid gets through a placental barrier.

The minimum daily need for ascorbic acid for the II-III trimesters of pregnancy – about 60 mg. It must be kept in mind that the fruit can adapt to high doses of ascorbic acid which is accepted by the pregnant woman, and then at the newborn development of an ascorbic disease as a syndrome of "cancellation" (at pregnancy it is not necessary to accept ascorbic acid in the raised doses, except for cases when the expected advantage for mother exceeds potential risk for a fruit) is possible.

The minimum daily requirement during breastfeeding – 80 mg. Ascorbic acid gets into breast milk therefore during feeding by a breast vitamin C is applied only under control of the doctor. Theoretically there is a danger to the child at use by mother of high doses of ascorbic acid (during feeding the breast does not recommend exceeding of daily need for ascorbic acid). In need of purpose of the raised doses of drug it is necessary to stop feeding by a breast.

Mother's diet containing adequate amount of ascorbic acid is sufficient for prevention of deficit of vitamin C at the baby.

Children.

Drug is used to children.


Overdose:

Symptoms: at single use of overdoses of drug developing of nausea, vomiting, swelling and abdominal pain, an itch, an enanthesis, a hyperexcitability is possible.
At intravenous administration in high doses there can be a threat of abortion.
Treatment. It is necessary to wash out a stomach, to give to the patient alkaline drink, absorbent carbon or other adsorbents. To carry out symptomatic therapy.

Storage conditions:

Period of validity. 2 years. To store in original packaging at a temperature from 2 °C to 8 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe


Packaging:

On 2 ml of solution for injections in an ampoule. On 5 ampoules in a blister strip packaging, on 2 blister strip packagings in a pack. On 10 ampoules in a box.



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