Pyridoxine hydrochloride

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT PYRIDOXINE HYDROCHLORIDE (PYRIDOXINE HYDROCHLORIDE)

Composition:

Active ingredient: pyridoxine hydrochloride;

1 ml of solution contains pyridoxine hydrochloride 50 mg;

Excipient: water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical properties: clear, colorless or slightly yellowish solution, practically free from particles.

Pharmaco-therapeutic group.

Simple vitamin preparations. Pyridoxine. ATC code A11HA02.

Pharmacological Properties.

Pharmacodynamics.

Pyridoxine hydrochloride (vitamin B6) is found in plants and animal organs, especially in unrefined cereal grains, vegetables, meat, fish, milk, liver of cod and cattle, and egg yolk. Yeast is also a rich source of vitamin B6. The requirement for vitamin B6 is met through food; partially, it is also synthesized by intestinal microflora.

It plays an important role in metabolism and is essential for the normal functioning of the central and peripheral nervous systems. It participates in the synthesis of neurotransmitters. In its phosphorylated form, it facilitates decarboxylation, transamination, and deamination of amino acids, participates in the synthesis of proteins, enzymes, hemoglobin, and prostaglandins, and is involved in the metabolism of serotonin, catecholamines, glutamic acid, gamma-aminobutyric acid (GABA), and histamine. It improves the utilization of unsaturated fatty acids, reduces cholesterol and lipid levels in the blood, enhances myocardial contractility, promotes the conversion of folic acid into its active form, and stimulates hematopoiesis. In atherosclerosis, vitamin B6 improves lipid metabolism.

Pyridoxine reduces the concentration of glycated hemoglobin in atherosclerosis and diabetes mellitus. Moreover, pyridoxine acts as a diuretic: it helps lower elevated arterial blood pressure.

It has been established that pyridoxine positively influences the production of norepinephrine and serotonin, increasing their synthesis in depression, which is related to its role as a cofactor of DOPA-decarboxylase in the synthesis of catecholamines.

Pyridoxine may prolong clotting time and inhibit platelet aggregation, which is explained by the binding of pyridoxal phosphate to fibrinogen and to specific amino groups on the surface of platelets.

Pharmacokinetics.

Metabolized in the liver to form pharmacologically active metabolites (pyridoxal phosphate and pyridoxamine phosphate). Pyridoxal phosphate is 90% bound to plasma proteins. It penetrates well into all tissues. It accumulates predominantly in the liver, to a lesser extent in muscles and the central nervous system. It crosses the placenta and is excreted in breast milk. The half-life period is 15–20 days. It is excreted by the kidneys; after intravenous administration, it is also excreted in bile (2%) and during hemodialysis.

Clinical characteristics.

Indications.

Hypo- and avitaminosis of vitamin B6. Complex treatment of toxemia in pregnancy, atherosclerosis, anemias (including sideroblastic anemia), leukopenias, nervous system disorders (radiculitis, neuritis, neuralgia, Parkinsonism, Little's disease), involutional depression, seborrheic and non-seborrheic dermatitis, herpes zoster, neurodermatitis, psoriasis, exudative diathesis, alcohol withdrawal and hangover syndrome. Also indicated for motion sickness (air and sea sickness), Meniere's disease. Pyridoxine hydrochloride prevents or reduces toxic effects (especially polyneuritis) during treatment with antituberculosis drugs. Treatment of pyridoxine-dependent seizures.

Contraindications.

Hypersensitivity to the components of the drug. Peptic ulcer disease of the stomach and duodenum (due to possible increase in gastric juice acidity); liver diseases associated with severe functional insufficiency; ischemic heart disease.

Interaction with other medicinal products and other types of interactions.

Diuretics – concomitant use with pyridoxine enhances the effect of diuretics.

Hormonal contraceptives, cycloserine, penicillamine, isoniazid, hydralazine sulfate, ethionamide, immunosuppressants – concomitant use with pyridoxine reduces the effect of the latter.

Sedatives and hypnotics – concomitant use with pyridoxine reduces hypnotic effect.

Antiparkinsonian agents – concomitant use with pyridoxine reduces the effectiveness of drugs used in Parkinson's disease treatment.

Phenytoin – concomitant use with pyridoxine reduces the effect of phenytoin.

Corticosteroids – concomitant use with pyridoxine decreases the amount of vitamin B6 in the body.

Glutamic acid, asparkam – concomitant use with pyridoxine increases resistance to hypoxia.

Cardiac glycosides – concomitant use with pyridoxine increases synthesis of contractile proteins in the myocardium.

Tricyclic antidepressants – concomitant use with pyridoxine alleviates side effects of tricyclic antidepressants related to their anticholinergic activity (dry mouth, urinary retention).

Resorptive-action chloramphenicol preparations – concomitant use with pyridoxine prevents ophthalmological complications arising from prolonged use of resorptive-action chloramphenicol preparations (sintomycin, chloramphenicol).

Special precautions for use.

Use with caution in patients with a history of peptic ulcer disease of the stomach and duodenum (due to possible increase in gastric acidity) and in patients with hepatic dysfunction (high-dose pyridoxine may worsen liver function).

Pyridoxine metabolism is impaired with regular alcohol consumption.

May lead to false-positive urobilinogen tests when using Ehrlich's reagent.

Use during pregnancy or breastfeeding.

The drug may be prescribed during pregnancy for pregnancy-related toxemia and vomiting in pregnancy. If the drug is administered during breastfeeding, suppression of lactation is possible.

Ability to influence reaction rate when driving or operating machinery.

During treatment, caution should be exercised when driving vehicles or operating complex machinery due to the possibility of adverse effects on the nervous system.

Administration and Dosage.

Pyridoxine hydrochloride is administered intramuscularly, intravenously, or subcutaneously in cases when oral administration is not possible.

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

The solution is prepared immediately before use—single dose of the drug is diluted in 1–2 mL of water for injections or 0.9% sodium chloride solution.

Adults.

Vitamin B6 deficiency: the drug is administered at a daily dose of 50–100 mg (1–2 mL) in 1–2 administrations. Treatment course: 3–4 weeks.

Sideroblastic anemia: the drug is administered intramuscularly at a daily dose of 100 mg (2 mL) twice a week. Concurrently, folic acid, riboflavin, and vitamin B12 are recommended.

Depression in involutional age: the drug is administered intramuscularly at a dose of 200 mg (4 mL) per day. Treatment course: 20–25 injections.

Use of isoniazid group drugs: the drug is administered at a daily dose of 5–10 mg (0.1–0.2 mL) throughout the entire course of isoniazid treatment.

Overdose of isoniazid group drugs: for each 1 g of overdosed drug, 1 g (20 mL) of pyridoxine is administered intravenously at a rate of 0.5 g/min. In case of isoniazid overdose exceeding 10 g, pyridoxine is administered intravenously at a dose of 4 g (80 mL), followed by intramuscular administration of 1 g (20 mL) every 30 minutes. Total daily dose: 70–350 mg/kg.

Pregnancy toxemia: the drug is administered intramuscularly at a dose of 50 mg (1 mL) per day. Treatment course: 10–20 injections.

Pyridoxine-dependent anemia (macrocytic, hypochromic with increased plasma iron levels): the drug is administered at a daily dose of 50–200 mg (1–4 mL). Treatment course: 1–2 months. If no effect is observed, alternative therapy is initiated.

Pyridoxine-dependent syndrome, including pyridoxine-dependent seizures: the drug is administered intravenously or intramuscularly at a dose of 50–500 mg (1–10 mL) per day. Intravenous administration is performed at a rate of 50 mg/min. Treatment course: 3–4 weeks.

Parkinsonism: the drug is administered intramuscularly at a dose of 100 mg (2 mL) per day. Treatment course: 20–25 days. After 2–3 months, a repeat course is administered. According to another treatment regimen:

the drug is administered intramuscularly at an initial daily dose of 50–100 mg (1–2 mL), then the dose is increased daily by 50 mg (1 mL) up to 300–400 mg (6–8 mL) per day as a single dose. Treatment is conducted in courses of 12–15 days.

Other indications: the drug is administered at a daily dose of 50–100 mg (1–2 mL) in 1–2 administrations.

Children.

Vitamin B6 deficiency: the physician prescribes the dose individually based on 1–2 mg/kg body weight per day. Treatment course: 2 weeks.

Pyridoxine-dependent seizures: the drug is administered intramuscularly or intravenously by slow bolus injection at a dose of 50–100 mg (1–2 mL) per day. Intravenous administration is performed at a rate of 50 mg/min. Maximum doses for children have not been established.

Overdose of isoniazid group drugs: for each 1 g of overdosed drug, 1 g (20 mL) of pyridoxine is administered intravenously. If the dose of isoniazid is unknown, pyridoxine is administered at a dose of 70 mg/kg body weight. Maximum dose: 5 g (100 mL).

Children.

The drug is used in pediatric practice. It is administered intramuscularly and intravenously. Dosage and administration regimen depend on the pathology (see section "Administration and Dosage").

Overdose.

Symptoms: exacerbation of adverse effects; disturbances in protein, carbohydrate, and lipid metabolism; degenerative changes in the central nervous system (peripheral neuropathy) and parenchymal organs (metabolic disturbances associated with a significant decrease in the activity of nicotinamide coenzymes NAD and NADP and niacin deficiency). Symptoms of peripheral neuropathy: hyperesthesia, paresthesia, muscle weakness. Sensory neuropathies may occur with progressive gait disturbance, numbness and tingling in the legs and arms, partial alopecia, decreased resistance to infections, and reduced activity of the blood coagulation system. With prolonged use in high doses, vitamin B6 hypervitaminosis develops, characterized by a sharp decrease in protein content in muscle and internal organs. Early signs of vitamin B6 hypervitaminosis may include skin rashes, dizziness, and seizures. These symptoms disappear after discontinuation of the drug.

Treatment: discontinuation of the drug; symptomatic therapy.

Adverse Reactions.

The following adverse reactions may occur during administration of pyridoxine hydrochloride:

Cardiovascular system: tachycardia, chest pain;

Central and peripheral nervous system: headache, dizziness, weakness, drowsiness, excitation, coordination disturbances, paresthesia, numbness in extremities, sensation of tightness in extremities – "gloves and socks" symptom, loss of consciousness and development of seizures with rapid intravenous administration;

Respiratory system: dyspnea;

Gastrointestinal tract: nausea, epigastric pain, heartburn, increased gastric secretion;

Metabolism and nutritional disorders: decreased folic acid levels;

Immune system, skin and subcutaneous tissue: hypersensitivity reactions, including anaphylactic shock, urticaria, rash, pruritus, skin hyperemia, dermatitis, Quincke's edema, photosensitization;

Reproductive system and mammary glands: inhibition of lactation during lactation period (sometimes used for therapeutic effect);

Local reactions at injection site: reactions at injection site, including hyperemia, pruritus, burning sensation at injection site;

General disorders: weakness, fever.

Shelf life. 3 years.

Storage conditions.

Store in original packaging at temperature not exceeding 25 °C.

Keep out of reach of children.

Incompatibility.

Do not mix pyridoxine solution in the same syringe with thiamine solution (vitamin B1), cyanocobalamin solution (vitamin B12), alkaline solutions, iron salts, or oxidizing agents. Pyridoxine injections should preferably be administered no earlier than 12 hours after thiamine injection.

It is not recommended to mix in the same infusion system or in the same syringe with the following medicinal products: adrenomimetics, sodium ampicillin, amphotericin B, ascorbic acid, other B-group vitamins, phytomenadione, dipyridamole, sodium oxiferroscorbide, phenothiazine derivatives (chlorpromazine), furosemide, etamsylate, euphyllin.

Packaging.

1 ml in an ampoule; 5 ampoules in a blister pack made of film, 1 or 2 blisters per cardboard box.

1 ml in an ampoule; 10 ampoules in a cardboard box with cardboard partitions.

Prescription category.

By prescription only.

Manufacturer.

JSC "Lubnipharm".

Manufacturer's address and location of business activity.

16, Barvinkova Street, Lubny, Poltava region, 37500, Ukraine.