Pyridoxine-darnitsya (vitamin b6-darnitsya)

INSTRUCTIONS FOR MEDICAL USE OF THE MEDICINAL PRODUCT PYRIDOXINE-DARNITSA (VITAMIN B6-DARNITSA) (PYRIDOXINE-DARNITSA (VITAMIN B6-DARNITSA))

Composition:

Active substance: pyridoxine hydrochloride;

1 ml of solution contains pyridoxine hydrochloride 50 mg;

Excipients: disodium edetate, water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: clear colorless or slightly colored liquid.

Pharmacotherapeutic group.
Simple vitamin preparations. Pyridoxine. ATC code A11HA02.

Pharmacological properties.

Pharmacodynamics.

Pyridoxine hydrochloride (vitamin B6) is present in plants and animal organs, particularly 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 dietary sources; additionally, it is partially synthesized by intestinal microflora.

It plays an essential role in metabolism and is necessary 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 processes of amino acids, participates in the synthesis of proteins, enzymes, hemoglobin, and prostaglandins, and is involved in the metabolism of serotonin, catecholamines, glutamic 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 level of glycated hemoglobin in atherosclerosis and diabetes mellitus. Furthermore, pyridoxine exerts a diuretic effect and helps lower elevated arterial 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 platelet surface.

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 and accumulates predominantly in the liver, to a lesser extent in muscles and the central nervous system (CNS). It crosses the placenta and is excreted into breast milk. The half-life (T1/2) is 15–20 days. It is excreted by the kidneys; after intravenous administration, approximately 2% is excreted via bile, and it is also removed during hemodialysis.

Clinical characteristics.

Indications.

Hypovitaminosis and avitaminosis of vitamin B6. Complex treatment of toxemia in pregnancy, atherosclerosis, anemias (including sideroblastic anemia), leukopenia, 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) and Meniere's disease. Pyridoxine hydrochloride prevents or reduces toxic effects (especially polyneuritis) during antituberculosis therapy. 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 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 pyridoxine.

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

Antiparkinsonian agents – concomitant use with pyridoxine decreases the effectiveness of drugs used to treat Parkinson's disease.

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 the synthesis of contractile proteins in the myocardium.

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

Resorbable chloramphenicol preparations – concomitant use with pyridoxine prevents ophthalmological complications arising from prolonged use of resorbable chloramphenicol preparations (synthomycin, 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 doses of pyridoxine may impair liver function).

Pyridoxine metabolism is impaired with regular alcohol consumption.

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

Use during pregnancy or breastfeeding.

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

Ability to influence reaction rate while driving or operating machinery.

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

Administration and Dosage.

Pyridoxine-Darnitsya is administered intramuscularly, intravenously, or subcutaneously when oral administration is not possible.

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

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

Adults.

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

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

Involutional depression: administer the drug intramuscularly at a dose of 200 mg (4 mL) per day. Treatment course: 20–25 injections.

Use of isoniazid group drugs: administer the drug 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, administer 1 g (20 mL) of pyridoxine intravenously at a rate of 0.5 g/min. In cases of isoniazid overdose exceeding 10 g, administer 4 g (80 mL) of pyridoxine intravenously, followed by 1 g (20 mL) intramuscularly every 30 minutes. Total daily dose: 70–350 mg/kg.

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

Pyridoxine-dependent anemia (macrocytic, hypochromic with elevated plasma iron levels): administer the drug at a daily dose of 50–200 mg (1–4 mL). Treatment course: 1–2 months. If no effect is observed, switch to another form of therapy.

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

Parkinsonism: administer the drug intramuscularly at a dose of 100 mg (2 mL) per day. Treatment course: 20–25 days. Repeat the course after 2–3 months. Alternatively: initiate treatment with an intramuscular daily dose of 50–100 mg (1–2 mL), increasing the dose daily by 50 mg (1 mL) until reaching 300–400 mg (6–8 mL) per day as a single dose. Treatment is administered in courses of 12–15 days.

Other indications: administer the drug at a daily dose of 50–100 mg (1–2 mL) given in 1–2 injections.

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: administer the drug intramuscularly or intravenously by slow bolus injection at a dose of 50–100 mg (1–2 mL) per day. When administered intravenously, the rate should be 50 mg/min. Maximum doses in children have not been established.

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

Children.

The drug can be used in pediatric practice. Administer intramuscularly or 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 NADPH and niacin deficiency). Symptoms of peripheral neuropathy include hyperesthesia, paresthesia, and muscle weakness. Sensory neuropathies may develop with progressive gait disturbance, numbness, and tingling in the arms and legs, partial alopecia, decreased resistance to infections, and reduced activity of the blood anticoagulant system. Long-term use in high doses leads to hypervitaminosis B6, characterized by a sharp decrease in protein content in muscle tissue and internal organs. Early signs of hypervitaminosis B6 may include skin rashes, dizziness, and seizures. Symptoms resolve upon discontinuation of the drug.

Treatment: discontinue the drug and provide symptomatic treatment.

Side effects

The following adverse reactions may occur with the use of this medicinal product:

Cardiovascular system: tachycardia, chest pain;

Central and peripheral nervous system: headache, dizziness, drowsiness, excitement, coordination disturbances, paresthesia, numbness in extremities, sensation of tightness in extremities – "glove and stocking" sensation, loss of consciousness and seizure development following 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, angioedema (Quincke's edema), photosensitization;

Reproductive system and mammary glands: suppression of lactation during lactation period;

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

General disorders: weakness, fever.

Shelf life. 3 years.

Storage conditions.

Store in the original packaging at a temperature not exceeding 25 °C. Do not freeze.

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 solutions. 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 syringe with the following medicinal products: adrenomimetics, ampicillin sodium, amphotericin B, ascorbic acid, other B-complex vitamins, phytomenadione, dipyridamole, sodium oxiferrosorbide, phenothiazine derivatives (chlorpromazine), furosemide, etamsylate, and ephedrine.

Packaging.

1 ml in an ampoule; 5 ampoules in a blister pack; 2 blisters per carton.

Prescription status. Prescription only.

Manufacturer.

JSC "Pharmaceutical Company "Darnytsia".

Manufacturer's address and place of business.

13, Boryspylska Street, Kyiv, 02093, Ukraine.