THIAMINE CHLORIDE-DARNYTSIA (VITAMIN B1-DARNYTSIA)

INSTRUCTION FOR MEDICAL USE OF THE MEDICINAL PRODUCT THIAMINE CHLORIDE-DARNITSA (VITAMIN B1-DARNITSA)

Composition:

Active substance: thiamine hydrochloride;

1 ml of solution contains thiamine hydrochloride 50 mg;

Excipients: unithiol, water for injections.

Pharmaceutical form. Injection solution.

Main physicochemical properties: clear colorless or slightly yellowish liquid with a weak characteristic odor.

Pharmacotherapeutic group. Simple vitamin B1 preparations. Thiamine (vitamin B1).

ATC code A11D A01.

Pharmacological properties.

Pharmacodynamics.

Thiamine chloride-Darnitsya is a synthetic vitamin B1 preparation belonging to water-soluble vitamins. In the human body, through phosphorylation processes, it is converted into cocarboxylase, which serves as a coenzyme for many enzymatic reactions. Vitamin B1 plays an essential role in metabolism and neuroreflex regulation, influences the conduction of nerve excitation in synapses, and exerts ganglion-blocking and curare-like effects. The drug may reduce the curare-like effect of depolarizing muscle relaxants.

Pharmacokinetics.

The drug is well absorbed. Phosphorylation occurs in the liver. It accumulates in the liver, heart, brain, kidneys, and spleen. It is excreted by the liver and kidneys; approximately 8–10% is excreted unchanged.

Clinical characteristics.

Indications.

Treatment of hypovitaminosis and avitaminosis B1, neuritis, polyneuritis, radiculitis, neuralgias, peripheral paralysis, encephalopathies, neurasthenia, peptic ulcer of the stomach and duodenum, intestinal atony, chronic liver disorders, myocardial dystrophy, endarteritis, neurogenic dermatoses, pyoderma, eczema, psoriasis.

Contraindications.

Hypersensitivity to the components of the drug; allergic diseases; idiosyncrasy; premenopausal and menopausal periods in women.

Interaction with other medicinal products and other types of interactions.

Concomitant use of the drug with other medicinal products may result in:

with depolarizing muscle relaxants (succinylcholine chloride), choline derivatives – reduced therapeutic effect;

with thiosemicarbazone, 5-fluorouracil – inhibition of thiamine activity;

with caffeine, drugs containing sulfur and estrogens – increased body demand for thiamine;

with anticonvulsants (phenobarbital, phenytoin, carbamazepine), digoxin, indomethacin, antacids – development of thiamine deficiency;

with cyanocobalamin, pyridoxine – impaired conversion of thiamine into phosphorylated biologically active form and enhanced allergizing effect. Concomitant parenteral administration of thiamine with pyridoxine (vitamin B6) or cyanocobalamin (vitamin B12) is not recommended;

with ethanol – slowed absorption rate of thiamine;

with adrenomimetics, sympathomimetics – reduced therapeutic effect.

When administered intravenously together with solutions containing sodium hydrosulfite as an antioxidant or preservative, thiamine is unstable.

Thiamine is unstable in alkaline and neutral solutions; co-administration with carbonates, citrates, barbiturates, Cu2+, iodide, iron-ammonium citrate, tannic acid is not recommended.

Special precautions for use.

Before parenteral administration of thiamine chloride solution, a skin test to determine individual sensitivity to the drug must be performed. After injection, monitoring for 30 minutes is required due to the possibility of severe allergic reactions.

Anaphylactic reactions occur more frequently after intravenous administration in high doses.

Thiamine injections should preferably be administered no sooner than 12 hours after pyridoxine injection.

For intramuscular administration, the drug should be injected deeply into the muscle; for intravenous administration, it should be given slowly.

Intramuscular and subcutaneous injections may be painful due to the low pH of the solution.

Daily requirement for vitamin B1: in adult males – 1.2–2.1 mg; in elderly individuals – 1.2–1.4 mg; in females – 1.1–1.5 mg, with an additional 0.4 mg for pregnant women and 0.6 mg for women during lactation; in children, depending on age – 0.3–0.5 mg.

The drug must not be used as a substitute for a balanced diet, but only as part of a comprehensive dietary therapy.

The injectable form of the drug should be used in treating patients with impaired intestinal absorption or following gastrectomy, when oral thiamine administration is not feasible (due to nausea, vomiting, pre- and postoperative periods), as well as in severe disease forms or at the beginning of treatment to achieve a therapeutic effect more rapidly.

Parenteral administration should be initiated with low doses (not more than 0.5 mL in adults), and higher doses should be administered only if the initial dose is well tolerated.

Use with caution in patients with increased nervous system excitability and hyperacidic forms of duodenal ulcer disease.

In Wernicke's encephalopathy, thiamine must be administered before glucose infusion.

If allergy to vitamin B1 is detected, the patient should avoid rice, buckwheat, meat, and bread (especially coarse flour varieties).

In patients with alcoholism, symptoms of adverse drug reactions may be intensified.

Thiamine may reduce the effectiveness of depolarizing muscle relaxants, adrenolytic agents, and sympathomimetic drugs.

The drug (when administered in high doses) may interfere with laboratory test results, causing false readings in spectrophotometric determination of theophylline in blood serum and in urobilinogen testing using Ehrlich's reagent.

Use during pregnancy or breastfeeding.

The drug may be used during pregnancy or breastfeeding when indicated and at recommended doses.

Ability to affect reaction speed when driving vehicles or operating machinery.

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

Method of Administration and Dosage.

Adults.

Administer the drug intramuscularly (deep into the muscle) at a dose of 25–50 mg (0.5–1 mL) once daily. Begin administration with low doses – no more than 25 mg (0.5 mL of a 5% solution); only if well tolerated, increase to higher doses – 50 mg (1 mL of a 5% solution). Treatment course: 10–30 injections.

Wernicke-Korsakoff encephalopathy: administer the drug intramuscularly (deep into the muscle) at a dose of 50–100 mg (1–2 mL of a 5% solution) twice daily until clinical improvement occurs. Be aware of the possibility of an allergic reaction to vitamin B1 administration.

Children aged 8 years and older: administer the drug at a dose of 12.5 mg (0.25 mL of a 5% solution) once daily. Treatment course: 10–30 injections.

Children.

For children, a 2.5% thiamine chloride solution is usually used. Administration of a 5% solution may be considered in children aged 8 years and older.

Overdose.

Symptoms: possible intensification of adverse drug reactions. Hypercoagulation and disturbances in purine metabolism may occur.

Treatment: discontinue the drug, symptomatic therapy.

Adverse reactions.

The following adverse reactions may occur during administration of the drug:

Cardiac disorders: tachycardia, palpitations;

Vascular disorders: collapse;

Nervous system disorders: headache, dizziness, anxiety, paresthesia;

Eye disorders: optic nerve damage;

Respiratory, thoracic and mediastinal disorders: dyspnea, shortness of breath;

Gastrointestinal disorders: dysphagia, nausea, intestinal hemorrhage;

Skin and subcutaneous tissue disorders: hyperemia, pruritus;

Immune system disorders: hypersensitivity reactions, including dermatitis, rash, urticaria, Quincke's edema, bronchospastic syndrome with convulsions, anaphylactic shock;

Hepatobiliary disorders: disturbances in liver enzyme activity;

General disorders and administration site conditions: increased sweating, chills, tremor, general weakness, edema, fever; injection site reactions, rash, pruritus;

synaptoplegia phenomenon – thiamine's ability to form complexes with various mediators may be accompanied by decreased arterial pressure, cardiac arrhythmias, impaired contraction of skeletal muscles (including respiratory muscles), and central nervous system depression; thiamine chloride promotes the development of staphylococcal resistance to antibiotics.

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.

Thiamine chloride should not be mixed in the same syringe with:

• benzylpenicillin or streptomycin, as this leads to destruction of antibiotics;
• nicotinic acid or solutions containing sulfites, as this leads to destruction of thiamine;
• carbonates, citrates, barbiturates, Cu2+, iodides, tannic acid, as thiamine is unstable in alkaline and neutral solutions.

Packaging.

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

Prescription status. Prescription only.

Manufacturer.

JSC "Pharmaceutical Company "Darnytsia".

Manufacturer's address and place of business.

13, Boryspylska Street, Kyiv, 02093, Ukraine.