Benzycillin-1 (Powder) Instructions for Use

ATC Code

J01CE08 (Benzathine benzylpenicillin)

Active Substance

Benzathine benzylpenicillin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Penicillin antibiotic, destroyed by penicillinase

Pharmacotherapeutic Group

Antibiotic, penicillin

Pharmacological Action

An antibiotic from the group of biosynthetic penicillins. The mechanism of antimicrobial action is based on the disruption of peptidoglycan synthesis – the muropeptide of the cell membrane, which leads to inhibition of the microorganism’s cell wall synthesis, suppression of the growth and reproduction of bacteria.

It is active against gram-positive bacteria, gram-negative cocci, Actinomyces spp., Spirochaetaceae.

It is inactive against strains of Staphylococcus spp. that produce penicillinase.

It has a prolonged action.

Pharmacokinetics

When administered intramuscularly, it is slowly absorbed from the injection site, providing a prolonged action. It penetrates the blood-brain barrier poorly. It is metabolized by hydrolysis to benzylpenicillin. Due to prolonged absorption, benzylpenicillin is detected in the urine for up to 12 weeks after a single dose administration.

Indications

Infectious and inflammatory diseases caused by pathogens sensitive to benzathine benzylpenicillin, including syphilis, yaws, pinta, acute tonsillitis, scarlet fever, erysipelas, wound infection; prevention of rheumatic fever exacerbations, scarlet fever (after contact with patients), erysipelas; prevention of infectious complications after tonsillectomy or tooth extraction.

ICD codes

Dosage Regimen

Administer the reconstituted suspension by deep intramuscular injection only. Do not administer intravenously, intra-arterially, or subcutaneously.

For adults, the single dose ranges from 300,000 IU to 2.4 million IU. For children, the single dose is 5,000 IU/kg to 10,000 IU/kg body weight. The maximum single dose for children should not exceed 1.2 million IU.

For treatment of syphilis (primary, secondary, latent early), administer a single dose of 2.4 million IU intramuscularly. For late latent syphilis and latent syphilis of unknown duration, administer 2.4 million IU once weekly for three consecutive weeks.

For prophylaxis of rheumatic fever, administer 1.2 million IU once every four weeks or 600,000 IU once every two weeks.

For treatment of streptococcal upper respiratory tract infections (e.g., tonsillitis, pharyngitis, scarlet fever), administer a single dose of 600,000 IU to 1.2 million IU for adults and 25,000 IU/kg to 50,000 IU/kg for children.

For prophylaxis of post-surgical infections (e.g., after tonsillectomy, tooth extraction), administer a single dose of 1.2 million IU for adults and a correspondingly lower dose for children prior to the procedure.

Adjust the frequency of administration and total duration of therapy based on the severity of the infection and the patient’s clinical response. The prolonged action of the drug allows for extended intervals between injections.

Adverse Reactions

From the hematopoietic system: anemia, thrombocytopenia, leukopenia, blood clotting disorders.

Effects due to chemotherapeutic action: with prolonged treatment, the development of superinfection with resistant microorganisms and fungi is possible.

Allergic reactions: urticaria, skin rash, rash on mucous membranes, fever, joint pain, eosinophilia, angioedema, erythema multiforme, exfoliative dermatitis, stomatitis, glossitis, in exceptional cases – anaphylactic and anaphylactoid reactions.

Contraindications

Hypersensitivity to benzathine benzylpenicillin and other antibiotics of the penicillin series.

Use in Pregnancy and Lactation

Benzathine benzylpenicillin crosses the placental barrier and is excreted in breast milk. Use during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.

If it is necessary to use during lactation, the issue of discontinuing breastfeeding should be decided.

Use in Renal Impairment

Use with caution in patients with impaired renal function.

Pediatric Use

Can be used in children according to indications.

Special Precautions

Use with caution in patients with impaired renal function, in case of a predisposition to allergic reactions (especially drug allergy), and with hypersensitivity to cephalosporins (due to the possibility of cross-allergy).

It is not recommended for the treatment of neurosyphilis (since the necessary plasma concentration is not achieved). Intravenous and endolumbar administration is not allowed.

Drug Interactions

With simultaneous use with NSAIDs (in particular, with indomethacin, phenylbutazone, and salicylates), the possibility of competitive inhibition of the excretion of drugs from the body should be considered.

In combination with bacteriostatically acting antibiotics, a decrease in the bactericidal effect of benzathine benzylpenicillin is noted.

Combination with other antibiotics is possible only with expected synergy of action.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.