Benzycillin-5 (Lyophilisate) Instructions for Use

Marketing Authorization Holder

Kraspharma, PJSC (Russia)

ATC Code

J01CE30 (Beta-lactamase-sensitive penicillins in combination)

Active Substances

Benzathine benzylpenicillin (Rec.INN registered by WHO)

Procaine benzylpenicillin (BAN adopted for use in the United Kingdom)

Dosage Form

Benzycillin-5

Lyophilisate for the preparation of suspension for intramuscular administration 1.2 million IU+300 thousand IU: fl. 1, 10 or 50 pcs.

Dosage Form, Packaging, and Composition

Vials.
Vials (10) – carton packs.
Vials (50) – carton boxes.

Clinical-Pharmacological Group

Penicillin antibiotic, destroyed by penicillinase

Pharmacotherapeutic Group

Antibiotic, penicillin

Pharmacological Action

A combined bactericidal antibiotic, consisting of two long-acting benzylpenicillin salts.

It suppresses the synthesis of the microorganism’s cell wall. Active against gram-positive microorganisms Staphylococcus spp. (non-penicillinase-producing), Streptococcus spp. (including Streptococcus pneumoniae), Corynebacterium diphtheriae, anaerobic spore-forming rods, Bacillus anthracis, Clostridium spp., Actinomyces israelii; gram-negative microorganisms Neisseria gonorrhoeae, Neisseria meningitidis, Treponema spp.

Strains of Staphylococcus spp. that produce penicillinase are resistant to the drug’s action.

Pharmacokinetics

After intramuscular administration of this combination, a high concentration of the antibiotic in the blood persists for up to 4 weeks.

Benzathine benzylpenicillin

After intramuscular injection, benzathine benzylpenicillin is hydrolyzed very slowly, releasing benzylpenicillin. C_max in blood serum is reached 12-24 hours after injection. The long T_1/2 provides a stable and long-lasting concentration of this active substance in the blood: on the 14th day after administration of a dose of 2,400,000 IU, the serum concentration is 0.12 mcg/ml; on the 21st day after administration of a dose of 1,200,000 IU – 0.06 mcg/ml (1 IU=0.6 mcg). Diffusion into fluids is complete, diffusion into tissues is very weak. Plasma protein binding is 40-60%. Benzathine benzylpenicillin penetrates the placental barrier in small amounts and is also excreted in breast milk. It is metabolized to a small extent. It is excreted mainly by the kidneys unchanged. Up to 33% of the administered dose is excreted within 8 days.

Procaine benzylpenicillin

C_max in blood plasma after intramuscular administration is reached in 20-30 minutes. T_1/2 is 30-60 minutes, in renal failure 4-10 hours or more. Plasma protein binding is 60%. It penetrates into organs, tissues and biological fluids, except for cerebrospinal fluid, eye tissues and prostate tissue. When the meningeal membranes are inflamed, it penetrates the blood-brain barrier. It penetrates the placental barrier and is excreted in breast milk. It is excreted by the kidneys unchanged.

Indications

Infectious and inflammatory diseases caused by susceptible pathogens: long-term (year-round) prevention of relapses of rheumatism; syphilis, yaws; streptococcal infections (excluding infections caused by group B streptococci) – acute tonsillitis, scarlet fever, wound infections, erysipelas.

ICD codes

Dosage Regimen

Administer by deep intramuscular injection into the upper outer quadrant of the gluteal muscle. Avoid intravenous, subcutaneous, intrathecal, or intra-arterial administration.

For adults, administer a single dose of 1.2 million IU benzathine benzylpenicillin and 300 thousand IU procaine benzylpenicillin once every 4 weeks.

For preschool children, administer a single dose of 480 thousand IU benzathine benzylpenicillin and 120 thousand IU procaine benzylpenicillin once every 3 weeks.

For children over 8 years of age, administer a single dose of 960 thousand IU benzathine benzylpenicillin and 240 thousand IU procaine benzylpenicillin once every 4 weeks.

Reconstitute the lyophilisate strictly according to the attached instructions using the provided sterile solvent. Shake the vial vigorously to form a uniform, opaque suspension immediately before administration.

For the long-term prevention of rheumatic fever recurrences, maintain the prescribed intervals between injections consistently.

When treating syphilis, perform microscopic and serological tests before initiating therapy and monitor for at least 4 months thereafter.

Adverse Reactions

Allergic reactions anaphylactic shock, anaphylactoid reactions, urticaria, fever, arthralgia, angioneurotic edema, multiform exudative erythema, exfoliative dermatitis.

Laboratory parameters anemia, thrombocytopenia, leukopenia, hypocoagulation.

Other stomatitis, glossitis.

Contraindications

Hypersensitivity to this combination, benzylpenicillin and other beta-lactam antibiotics; breastfeeding period.

With caution

Pregnancy, renal failure, burdened allergic history, bronchial asthma, pseudomembranous colitis.

Use in Pregnancy and Lactation

Use during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus.

Contraindicated for use during breastfeeding.

Use in Renal Impairment

Use with caution in renal failure.

Pediatric Use

Used according to indications

Special Precautions

Do not administer subcutaneously, intravenously, endolumbally, or into body cavities.

In case of accidental intravascular injection, transient feelings of depression, anxiety and visual disturbances (Hoigne’s syndrome) may occur.

When treating syphilis, microscopic and serological tests should be performed before starting therapy and then for 4 months.

Due to the development of fungal infections, it is advisable to simultaneously prescribe B vitamins and vitamin C, and if necessary, systemic antifungal drugs. It must be taken into account that the use of insufficient doses or too early discontinuation of treatment often leads to the emergence of resistant strains of pathogens.

Drug Interactions

Bactericidal antibiotics (including cephalosporins, vancomycin, rifampicin, aminoglycosides) have a synergistic effect; bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines) have an antagonistic effect.

Increases the effectiveness of indirect anticoagulants (by suppressing intestinal flora, reduces the prothrombin index); reduces the effectiveness of oral contraceptives, drugs in the metabolism of which para-aminobenzoic acid is formed, ethinylestradiol – the risk of “breakthrough” bleeding.

Diuretics, allopurinol, tubular secretion blockers, phenylbutazone, NSAIDs, by reducing tubular secretion, increase the concentration of benzylpenicillin in the blood and tissues.

Allopurinol increases the risk of allergic reactions (skin rash).

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.