Pyridoxine hydrochloride (B6 Vitamin)

General characteristics. Structure:

Active agent – a pyridoxine a hydrochloride and (in terms of 100% substance) – 50 mg.

Excipients: water for injections.

Pharmacological properties:

Pharmacokinetics. The pyridoxine is well soaked up at introduction inside, and vitamin B absorption process a small intestine happens by passive diffusion and is not saturable. Normal concentration of a pyridoxine in a blood plasma make 3-18 mg/ml. In blood it is transported in the state connected with albumine and hemoglobin of erythrocytes. In a liver the pyridoxine turns into 3 vitamer who are capable to pass mutually each other: pyridoxine, пиридоксаль and pyridoxamine. The main depot of a pyridoxine in an organism are skeletal muscles which contain 80-90% of all pyridoxine of an organism. Removal of a pyridoxine happens to urine in the form of inactive piridoksovy acid. The period of semi-elimination makes 25-33 days.

Pharmacodynamics. A pyridoxine the hydrochloride concerns to group of water-soluble vitamins (B6 vitamin). Fills shortage of B6 vitamin, exerts the regulating impact on exchange of amino acids, neurotransmitters.

The pyridoxine is a coenzyme of transaminases and decarboxylases which provide exchange of amino acids and synthesis of neurotransmitters.

In muscles (including in a myocardium) the pyridoxine activates processes of disintegration of a glycogen and optimizes energy balance of muscles in the conditions of a hypoxia. Provides synthesis of niacin (RR vitamin) from tryptophane. Regulates exchange of glutaminic acid, methionine, cysteine.

In a nervous system the pyridoxine participates in synthesis of neurotransmitters: noradrenaline, dopamine, glycine, GAMK and serotonin. At the same time it changes balance of the specified mediators towards dominance of brake mediators – GAMK, glycine, and also serotonin. Thus, the pyridoxine takes part in regulation of excitability of the central nervous system (CNS). The pyridoxine activates anti-nociceptive system and strengthens action of analgeziruyushchy means.

Stimulates synthesis gem in hemoglobin, increases synthesis of iron-binding protein of marrow (siderophilin), regulates exchange of B12 vitamin and folic acid. Contacting the lysine remains on a surface of thrombocytes and fibrinogen, causes delay of coagulability of blood and aggregation of thrombocytes, improves the flowability of blood and blood supply of fabrics.

The pyridoxine modifies, effect of steroid hormones: estrogen, androgens, gestagen, glucocorticosteroid hormones, changing a vzamodeystviye hormone - a receptor complex with a cell kernel.

Indications to use:

- B6 hypovitaminosis

- toxicoses of pregnant women, intolerance of the combined oral contraceptives

- hypochromia sideroakhristichesky (sideroblastny) anemia

- a pyridoxine - a dependent convulsive syndrome at children

- neurotoxic action of an isoniazid, gidralazin, Cycloserinum and D-Penicillaminum (treatment and prevention)

- diseases of a nervous system (Littl's disease, a hysterical chorea, neuralgia and neuritis) as a part of complex therapy

- Menyer's disease, sea and aeroembolism

- seboreepodobny and not seborrheal dermatitis, neurodermatitis, psoriasis, exudative diathesis.

Route of administration and doses:

Appoint a pyridoxine subcutaneously, intramusculary or intravenously.

Medical doses parenterally (under skin, intramusculary and intravenously) enter the adult 0,05 - 0,1 g a day (1-2 ml of 5% of solution into 1-2 receptions), to children - on 0,02-0,025 g (0,5 ml of 5% of solution of 1 times a day). A course of treatment for adults 1 month, for children - 2 weeks.

The daily need for a pyridoxine for adult men makes 2 mg, for women - 2 mg and in addition at pregnancy - 0,3 mg, when feeding by a breast - 0,5 mg, for children and teenagers depending on age – 0,4-2 mg.

Features of use:

Pregnancy and lactation. The pyridoxine gets through a placenta and is allocated in maternal milk. Use of a pyridoxine in high doses during pregnancy and a lactation can lead to development of "pyridoxynew dependence" in children. It is not recommended to exceed standards of physiological need for a pyridoxine during pregnancy (2-2,3 mg/days). The pyridoxine strengthens synthesis of dopamine in TsNS (which carries out a pro-lactostatine role) and can stop a lactation at nursing mothers.

Use with care. It is necessary to be careful at purpose of a pyridoxine to patients with a peptic ulcer of a stomach and duodenum, an ischemic heart disease since administration of drug can provoke an exacerbation of a disease.

Use of a pyridoxine does not affect ability of the patient to control of the vehicle or other operator activity.

Side effects:

- allergic reactions (including acute anaphylaxis)

- irritation of a mucous membrane of a stomach, abdominal pain

- a syndrome of "pyridoxynew dependence" at long introduction of a pyridoxine in a dose of 100-200 mg/days. It is characterized seborrheas, a glossitis, confusion of consciousness, a growth inhibition and development, by anemia, spasms.

Interaction with other medicines:

Weakens neurotoxic action of an isoniazid, gidralazin, Cycloserinum and D-Penicillaminum.

The pyridoxine weakens protivoparkinsonichesky activity of a levodopa, accelerating processes of her metabolism in digestive tract and a liver that interferes with receipt of a levodopa in TsNS.

Promotes digestion of iron and its deposition in got into condition.

Strengthens effects of indirect anticoagulants (Fenindionum, warfarin, neodicoumarin) and heparin.

Strengthens analgetic effect of metamizol (analginum), acetylsalicylic acid, a tramadol and nefopam.

Pharmaceutical it is incompatible with B1 and B12 vitamins.

Contraindications:

- hypersensitivity to a pyridoxine

- end-stage of a liver failure

- children's age up to 2 years

Overdose:

Symptoms of overdose arise at introduction of a pyridoxine in high doses (200-2000 mg/days and more). Development of numbness of brushes and feet, emergence of feeling of a prelum in them is characteristic.

Treatment symptomatic therapy (introduction of small doses of a neostigmin or Galantaminum for improvement of neuro and muscular transfer). There is no specific antidote.

Storage conditions:

In the dry, protected from light place, at a temperature not over 30 ºС.

To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

On 1 ml in ampoules of neutral glass.

On 10 ampoules place in a box from a cardboard.

On 5 or 10 ampoules pack into a blister strip packaging.

On 2 planimetric packagings No. 5 together with the application instruction place in a pack from a cardboard.