Pyridoxine of girokhlorid-Darniyets (B6 vitamin)

General characteristics. Structure:

Active ingredient: pyridoxine;

1 ml of solution contains a pyridoxine of a hydrochloride 50 mg;

excipients: dinatrium эдетат, water for injections.

Pharmacological properties:

Pharmacodynamics. A pyridoxine the hydrochloride (B6 vitamin) contains in plants and bodies of animals, especially in the crude grains of cereal cultures, in vegetables, meat, fish, milk, cod liver and cattle, an egg yolk. A lot of B6 vitamin contains in yeast. The need for B6 vitamin is satisfied with food stuffs; partially it is synthesized also by intestinal microflora.

Plays an important role in a metabolism, it is necessary for normal functioning of the central and peripheral nervous system, participates in synthesis of neurotransmitters. In a fosforilirovanny form provides processes of decarboxylation, interamination, deamination of amino acids, participates in synthesis of protein, enzymes, hemoglobin, prostaglandins, exchange of serotonin, catecholamines, glutaminic acid, GAMK, histamine, improves use of unsaturated fatty acids, reduces the level of cholesterol and lipids in blood, improves contractility of a myocardium, promotes transformation of folic acid into its active form, stimulates a hemogenesis. At atherosclerosis B6 vitamin improves lipidic exchange.

The pyridoxine at atherosclerosis and a diabetes mellitus reduces the content of glikozilirovanny hemoglobin, besides, the pyridoxine works as diuretic: helps to reduce the increased arterial pressure.

It is established that the pyridoxine positively influences development of Norepinephrinum and serotonin, raising their products at depressions that is connected with its participation as a dofa-decarboxylase cofactor in the course of synthesis of catecholamines.

The pyridoxine can increase time of coagulation and inhibit aggregation of thrombocytes that is probably explained by linkng of pyridoxal phosphate with fibrinogen and with specific amino groups a surface of thrombocytes.

Pharmacokinetics. It is metabolized in a liver with formation pharmacological of active metabolites (pyridoxal phosphate and пиридоксаминофосфат). Pyridoxal phosphate contacts proteins of plasma for 90%. Well gets into all fabrics. Collects preferential in a liver, it is less – in muscles and TsNS. Gets through a placenta, it is excreted in breast milk. Time of semi-removal (T1/2) – 15-20 days. It is removed by kidneys (at intravenous administration – with bile (2%), and also during a hemodialysis.

Pharmaceutical characteristics.

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

Indications to use:

Hypo - and B6 vitamin avitaminosis. Complex treatment of toxicosis of pregnant women, atherosclerosis, anemias (including sideroblastny), leukopenias, diseases of a nervous system (radiculitises, neuritis, neuralgia, parkinsonism, Littl's disease), depressions of involutional age, acute and chronic hepatitises, seboreepodobny and not seborrheal dermatitis, shingles, neurodermatitis, psoriasis, exudative diathesis, at removal from hard drinking and a hangover syndrome. Appoint also at air and sea diseases, Menyer's disease. A pyridoxine the hydrochloride warns or reduces toxic effects (especially polyneurites) at treatment by antitubercular drugs. Treatment of piridoksinzavisimy spasms.

Route of administration and doses:

The drug Piridoksin-Darnitsa is administered intramusculary, intravenously or subcutaneously in cases when oral administration is impossible.

The course of treatment is individual and is defined by type and disease severity.

Solution is prepared just before use – the single dose of drug is parted in 1-2 ml of water for injections or 0,9% chloride sodium solution.

 

Adult.

B6 hypovitaminosis: drug appoint in a daily dose 50-100 mg (1-2 ml) for 1-2 introductions. A course of treatment – 3-4 weeks.

Sideroblastny anemia: drug is appointed intramusculary in a daily dose of 100 mg (2 ml) by 2 times a week. It is at the same time recommended to accept folic acid, Riboflavinum, B12 vitamin).

Depressions of involutional age: drug is appointed intramusculary in a dose of 200 mg (4 ml) in days. A course of treatment – 20-25 injections.

Use of drugs of group of an isoniazid: drug appoint in a daily dose 5-10 mg (0,1-0,2 ml) during all course of treatment an isoniazid.

Overdose of drugs of group of an isoniazid: on each 1 g of the overdosed drug enter intravenously 1 g (20 ml) of a pyridoxine with a speed of 0,5 g/min. At overdose of an isoniazid over 10 g enter a pyridoxine intravenously in a dose of 4 g (80 ml), and then intramusculary – on 1 g (20 ml) of drug each 30 minutes. The general daily   dose – 70-350 mg/kg.

Toxicosis of pregnant women: drug is appointed intramusculary in a dose of 50 mg (1 ml) in days. A course of treatment – 10-20 injections.

Piridoksinzavisimy anemia (gland, macrocytic, hypochromia with increase in level, in a blood plasma): drug appoint 50-200 mg (1-4 ml) in a daily dose. A course of treatment – 1-2 months. In case of lack of effect pass to other type of therapy.

Piridoksinzavisimy syndrome, including piridoksinzavisimy spasms: drug is appointed intravenously or intramusculary in a dose of 50-500 mg (1-10 ml) in days. Intravenously enter with a speed of 50 mg/min. A course of treatment – 3-4 weeks.

Parkinsonism: drug is appointed intramusculary in a dose of 100 mg (2 ml) in days. A course of treatment – 20-25 days. In 2-3 months – a repeated course. According to other scheme of treatment: drug is appointed intramusculary in an initial daily dose of 50-100 mg (1-2 ml), and then daily the dose is increased by 50 mg (1 ml) and brought to 300-400 mg (6-8 ml) a day one-time. Treatment is performed by courses in 12-15 days.

Other indications: drug appoint in a daily dose 50-100 mg (1-2 ml) for 1-2 introductions.

To children.

B6 hypovitaminosis: the doctor appoints a drug dose individually at the rate of 1-2 mg/kg of body weight a day. A course of treatment – 2 weeks.

Piridoksinzavisimy spasms: drug is appointed intramusculary or intravenously struyno in a dose of 50-100 mg (1-2 ml) in days. Intravenously enter with a speed of 50 mg/min. The maximum doses for children are not established.

Overdose of drugs of group of an isoniazid: on each 1 g of the overdosed drug enter intravenously 1 g (20 ml) of a pyridoxine. If the dose of an isoniazid is unknown, the pyridoxine is entered at the rate of 70 mg/kg of body weight. The maximum dose – 5 g (100 ml).

Features of use:

Use during pregnancy or feeding by a breast.

Drug is appointed during pregnancy at toxicosis of pregnant women and at vomiting of pregnancy. At purpose of drug during feeding by a breast oppression of a lactation is possible.

Children.

Drug is used in pediatric practice. Enter intramusculary and intravenously. Doses and the mode of introduction depend on pathology  (see the section "Route of Administration and Doses").

To apply with care to patients with a peptic ulcer of a stomach and duodenum in the anamnesis (because of possible increase in acidity of a gastric juice), at a functional hepatic unsufficiency (the pyridoxine in high doses can worsen its function).

Exchange of a pyridoxine is broken at regular alcohol intake.

Can lead to false positive test on urobilinigen with use of a reactant of Ehrlich.

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

During treatment it is necessary to be careful at control of vehicles and work with difficult mechanisms in connection with a possibility of development of side effects from a nervous system.

Side effects:

At use of drug the following side reactions are possible:

from cardiovascular system: tachycardia, pain in heart;

from the central and peripheral nervous system: a headache, dizziness, drowsiness, excitement, a lack of coordination, paresthesias, numbness in extremities, emergence of feeling of compression in extremities – a symptom "stockings and gloves", a loss of consciousness and development of spasms at bystry intravenous administration;

from respiratory system: the complicated breath;

from digestive tract: nausea, pain in epigastric area, heartburn, increase in gastric secretion;

from a metabolism, metabolism: decrease in level of folic acid;

from immune system, skin and hypodermic cellulose: acute anaphylaxis, small tortoiseshell, rashes, itch, dermahemia, dermatitis, Quincke's edema, photosensitization;

from reproductive system and mammary glands: oppression of a lactation during the lactogenic period (sometimes use for medical effect);

disturbances in an injection site: changes in an injection site, including a hyperemia, an itch, burning in the place of injections;

general disturbances: weakness, fever.

Interaction with other medicines:

Diuretics – at the combined use with a pyridoxine effect of diuretics amplifies.

Hormonal contraceptives, Cycloserinum, Penicillaminum, isoniazid, gidralazin sulfate, Etioniamidum, immunnodepressant – at the combined use with a pyridoxine decreases effect of the last.

Somnolent and sedative means – at the combined use with a pyridoxine the somnolent effect is weakened.

Protivoparkinsonichesky means – at the combined use with a pyridoxine efficiency of means for treatment of a disease of Parkinson decreases.

Phenytoinum – at the combined use with a pyridoxine is weakened action of Phenytoinum.

Corticosteroids – at the combined use with a pyridoxine the amount of B6 vitamin in an organism decreases.

Glutaminic acid, asparkam – at the combined use with a pyridoxine raises resistance to a hypoxia.

Cardiac glycosides – at the combined use with a pyridoxine synthesis of sokratitelny proteins in a myocardium increases.

Tricyclic antidepressants – at the combined use with a pyridoxine the last eliminates the side effects of tricyclic antidepressants connected with their anticholinergic activity (dryness in a mouth, an ischuria).

Drugs of levomycetinum of resorptive action – at the combined use with a pyridoxine the last warns ophthalmologic complications which arise at prolonged use of drugs of levomycetinum of resorptive action (synthomycin, chloramphenicol).

Contraindications:

Hypersensitivity to drug components. A peptic ulcer of a stomach and duodenum (in connection with possible increase in acidity of a gastric juice). The liver diseases proceeding with heavy functional insufficiency. Coronary heart disease.

Overdose:

Simptomy:usileniye of side effects; disturbance of exchange of proteins, carbohydrates and lipids; degenerative changes in the central nervous system (peripheral neuropathy) and parenchymatous bodies (the disturbance of processes of exchange connected with considerable decrease of the activity of nikotinamidny coenzymes of NAD and NADF and deficit of niacin). Symptoms of peripheral neuropathy: hyper paresthesias, paresthesias, muscular weakness. Partial baldness, decrease in body resistance to infections, decrease of the activity of anticoagulative system of blood are possible touch neuropathy with the progressing walking disturbance, feeling of numbness and a pricking in legs and hands. At prolonged use in high doses the hypervitaminosis of B6 which is characterized by sharp decrease in protein content in muscular tissue and internals develops. At early stages of a hypervitaminosis of B6 can appear: rash on skin, dizziness, spasms. At drug withdrawal these symptoms disappear.

Treatment. Drug withdrawal, symptomatic treatment.

Storage conditions:

Period of validity. 3 years. To store in the place, unavailable to children, in original packaging at a temperature not above 25 °C. Not to freeze.

Issue conditions:

According to the recipe

Packaging:

On 1 ml in an ampoule; on 10 ampoules in a box; on 10 ampoules in a blister strip packaging; on 1 blister strip packaging in a pack; on 5 ampoules in a blister strip packaging; on the 2nd blister strip packagings in a pack.