BINAVIT^® forte (Tablets) Instructions for Use

Marketing Authorization Holder

Binergia JSC (Russia)

Manufactured By

PharmVILAR NPO, LLC (Russia)

ATC Code

A11DB (Vitamin B1 in combination with vitamins B6 and/or B12)

Active Substances

Cyanocobalamin (Rec.INN registered by WHO)

Pyridoxine (Rec.INN registered by WHO)

Thiamine (Rec.INN registered by WHO)

Dosage Form

BINAVIT® forte

Film-coated tablets, 200 mg+100 mg+0.2 mg: 20 or 60 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or almost white, round, biconvex; on the cross-section, the core is from white to light pink with inclusions from light pink to dark pink.

* (calculated as 100% substance).

Excipients: microcrystalline cellulose 102 – 80 mg, magnesium stearate – 4.8 mg, povidone K30 – 15 mg.

Shell composition: macrogol 6000 – 9 mg, titanium dioxide – 13.5 mg, talc – 30 mg, hypromellose – 7.5 mg.

10 pcs. – blister packs (2) – cardboard packs.
10 pcs. – blister packs (6) – cardboard packs.

Clinical-Pharmacological Group

B complex vitamins

Pharmacotherapeutic Group

Vitamins; vitamin B1 and its combinations with vitamins B6 and B12; vitamin B1 in combination with vitamins B6 and/or B12

Pharmacological Action

The pharmacological action is determined by the properties of the vitamins that make up the drug.

The drug contains vitamins B₁ (thiamine), B₆ (pyridoxine) and B₁₂ (Cyanocobalamin), the deficiency of which can lead to neurological disorders, mainly from the peripheral nervous system.

Neurotropic B vitamins have a beneficial effect on inflammatory and degenerative diseases of the nerves and locomotor apparatus, contribute to increased blood flow and improve the functioning of the nervous system.

Thiamine is a cofactor of enzymes that transfer two-carbon groups in decarboxylation reactions, plays a key role in carbohydrate metabolism, as well as in the Krebs cycle with subsequent participation in the synthesis of thiamine pyrophosphate (TPP) and ATP.

Pyridoxine is a cofactor of transaminases, participates in protein metabolism and, partially, in the metabolism of carbohydrates and fats.

The physiological function of both vitamins is to potentiate each other’s action, manifested in a positive effect on the nervous, neuromuscular and cardiovascular systems.

Cyanocobalamin is a cofactor in one-carbon group transfer reactions, participates in the synthesis of the myelin sheath, stimulates hematopoiesis, reduces pain associated with damage to the peripheral nervous system, stimulates nucleic acid metabolism through the activation of folic acid.

The drug quickly replenishes the deficiency of these vitamins.

Pharmacokinetics

Thiamine

After oral administration, thiamine undergoes dose-dependent transport, the mechanism of which is dual in nature: active absorption at concentrations up to 2 µmol/L and passive diffusion at concentrations above 2 µmol/L. Phosphorylation of thiamine occurs in the liver. T_1/2 is about 4 hours.

The human body contains about 30 mg of thiamine. Given the rapid metabolism, it is eliminated within 4-10 days.

Pyridoxine

Pyridoxine is absorbed very quickly, mainly in the upper intestine, and is eliminated within a maximum of 2-5 hours. Pyridoxine in phosphorylated form (pyridoxal phosphate) is almost 80% bound to plasma proteins. The human body contains about 40-150 mg of pyridoxine. The kidneys excrete 1.7-3.6 mg per day.

Cyanocobalamin

Cyanocobalamin is absorbed from the gastrointestinal tract through 2 mechanisms

• Release under the action of gastric juice and rapid binding to intrinsic factor;
• Passive diffusion through the intestinal epithelium regardless of intrinsic factor.

At doses above 1.5 mcg, the latter mechanism plays a significant role.

In patients with B₁₂-deficiency anemia, reabsorption after oral administration is approximately 1% from 100 mcg and above.

Excess cyanocobalamin mainly accumulates in the liver.

From the liver, it is excreted with bile into the intestine and is significantly reabsorbed during enterohepatic circulation. The rate of cyanocobalamin metabolism per day is 2.5 mcg.

Indications

As part of complex therapy for the following neurological diseases accompanied by B vitamin deficiency

• Polyneuropathy (diabetic, alcoholic);
• Intercostal neuralgia;
• Trigeminal neuralgia;
• Facial nerve neuritis;
• Radicular syndrome caused by degenerative changes of the spine;
• Cervical syndrome;
• Shoulder-scapular syndrome;
• Lumbar syndrome;
• Lumbosciatica.

ICD codes

Dosage Regimen

Take the tablets after meals to minimize potential gastrointestinal discomfort.

Swallow the tablet whole; do not chew or crush it.

Take with a small amount of water.

The standard dosage for adults is 1 tablet 1 to 3 times daily.

The exact frequency and duration of therapy must be determined by a physician based on the specific neurological condition and its severity.

Adhere strictly to the treatment duration prescribed by your doctor.

Do not use high doses of the drug for a period exceeding 4 weeks.

For any long-term therapy, your physician should regularly monitor your clinical status.

Discontinue use and consult your doctor immediately if symptoms of peripheral sensory neuropathy, such as numbness or tingling, occur.

Avoid concurrent use of other multivitamin complexes containing B vitamins.

Adverse Reactions

The frequency of adverse events is given in accordance with the WHO classification: very common (≥1/10); common (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rare (≥1/10000, <1/1000); very rare (<1/10000), including isolated cases; frequency unknown (cannot be estimated from the available data).

From the immune system very rare – allergic reactions, incl. urticaria, itching.

From the gastrointestinal tract frequency unknown – nausea.

From the cardiovascular system very rare – tachycardia.

Contraindications

• Hypersensitivity to the components of the drug;
• Childhood (the efficacy and safety of the drug have not been studied);
• Severe and acute forms of decompensated chronic heart failure (CHF);
• Pregnancy;
• Breastfeeding period.

Use in Pregnancy and Lactation

Use during pregnancy and breastfeeding is contraindicated.

Pediatric Use

Use in children is contraindicated.

Special Precautions

With long-term use (more than 6-12 months) of vitamin B₆ at a daily dose of 50 mg, peripheral sensory neuropathy may occur. Therefore, during long-term therapy, it is recommended to regularly monitor the patient’s condition.

If signs of peripheral sensory neuropathy (paresthesia) appear, it is necessary to adjust the dose and, if necessary, discontinue the drug.

When taking vitamin B₁₂, the clinical picture, as well as laboratory parameters in funicular myelosis or pernicious anemia, may lose their specificity. Vitamin B₁₂ may mask the symptoms of folic acid deficiency.

During the use of Binavit forte, it is not recommended to take multivitamin complexes that include B vitamins.

Effect on ability to drive vehicles and machinery

Binavit forte does not affect the ability to drive vehicles and machinery.

Overdose

Clinical symptoms of an overdose of the vitamins contained in Binavit forte can be expected only after taking extremely high doses for a very long time.

Vitamin B₁

Thiamine has a wide therapeutic range. Very high doses (>10 g) have a ganglion-blocking effect and suppress the transmission of nerve impulses, i.e., have a muscle relaxant effect.

Vitamin B₆

Pyridoxine has very low toxicity.

The use of pyridoxine for 2 months or more at a dose of more than 1 g/day can cause neurotoxic effects.

After oral administration of more than 2 g/day, the following effects were noted: neuropathies with ataxia, sensory disturbances, cerebral convulsions with ECG changes, and, in some cases, hypochromic anemia and seborrheic dermatitis.

Vitamin B₁₂

After parenteral administration of a high dose (as well as in rare cases after oral administration), eczematous skin changes and a benign form of acne were observed.

Treatment: gastric lavage, administration of activated charcoal, prescription of symptomatic therapy.

Drug Interactions

When used concomitantly with levodopa, pyridoxine may reduce the antiparkinsonian effect of levodopa.

Concomitant use of pyridoxine antagonists (e.g., isoniazid, hydralazine, penicillamine, or cycloserine) may increase the need for pyridoxine.

Thiamine is inactivated by fluorouracil. Fluorouracil competitively inhibits the phosphorylation of thiamine to thiamine pyrophosphate.

Antacids reduce the absorption of thiamine.

“Loop” diuretics, e.g., furosemide, can block tubular reabsorption, thus enhancing the excretion of thiamine during long-term use, which leads to a decrease in thiamine levels in the blood.

Ethanol and black tea lead to reduced absorption of thiamine.

Beverages containing sulfites (e.g., wine) enhance the degradation of thiamine.

Storage Conditions

The drug should be stored out of the reach of children, protected from light, at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years. Do not use after the expiration date printed on the packaging.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.