Benzycillin-3 (Powder) Instructions for Use

ATC Code

J01CE30 (Beta-lactamase-sensitive penicillins in combination)

Active Substances

Benzathine benzylpenicillin (Rec.INN registered by WHO)

Benzylpenicillin (Rec.INN registered by WHO)

Procaine benzylpenicillin (BAN adopted for use in Great Britain)

Clinical-Pharmacological Group

Penicillin antibiotic, destroyed by penicillinase

Pharmacotherapeutic Group

Antibiotic, penicillin

Indications

• Infections caused by microorganisms highly sensitive to benzylpenicillin: This includes streptococcal infections (excluding those caused by enterococci), including streptococcal tonsillopharyngitis.
• Syphilis: All stages of infection caused by Treponema pallidum.
• Yaws: Treatment of the tropical infection caused by Treponema pallidum subspecies pertenue.
• Prevention of rheumatic fever: Secondary prophylaxis for the prevention of recurrent attacks in patients with a history of rheumatic fever or rheumatic heart disease.

The use of the drug is justified only when the causative agent of the infection is sensitive to the active substances of the drug. The combination of salts provides both an immediate therapeutic effect (benzylpenicillin sodium salt) and a prolonged, sustained antibacterial effect (benzathine benzylpenicillin and procaine benzylpenicillin).

Contraindications

• Hypersensitivity: A history of severe hypersensitivity reactions (e.g., anaphylaxis, angioedema, severe skin reactions) to any penicillin antibiotic, other beta-lactam antibiotics (such as cephalosporins, carbapenems, monobactams), or to procaine.
• Severe Renal Impairment: The use of the drug is contraindicated in patients with severe renal failure (creatinine clearance less than 10 ml/min) due to the increased risk of neurotoxicity from accumulated penicillins.
• Epilepsy and Other CNS Disorders: The drug is contraindicated in patients with a history of epilepsy or other conditions predisposing to seizures, as high doses of penicillins can lower the seizure threshold.
• Intrathecal Administration: Under no circumstances should Benzycillin-3 be administered intrathecally, as this can lead to severe and potentially fatal neurotoxic reactions.
• Concomitant Use with Disulfiram: Contraindicated in patients receiving or having recently received disulfiram, due to the risk of acute psychotic reactions and other adverse interactions related to the procaine component.

The presence of any of these conditions requires the selection of an alternative antibacterial therapy that is safe for the patient.

Dosage Regimen

The dosage of Benzycillin-3 is set individually by the physician, depending on the severity, localization of the infection, and the sensitivity of the pathogen. The drug is intended for deep intramuscular injection only; intravenous, subcutaneous, or intra-arterial administration is strictly prohibited.

Preparation of Suspension: The contents of the vial are dissolved in 2-4 ml of sterile water for injection or 0.9% sodium chloride solution immediately before administration. The suspension is shaken vigorously until a homogeneous, cloudy liquid is formed. The prepared suspension is not intended for storage and must be used immediately.

For adults and children over 12 years of age, the usual dose is 1.2 million IU once every 3-4 days. For the treatment of primary and secondary syphilis, a course of 6-8 injections is recommended. For tertiary and latent syphilis, the course is extended. For the prevention of rheumatic fever, 1.2 million IU is administered once every 3-4 weeks.

For children under 12 years of age, the dose is calculated individually based on body weight and the severity of the infection, typically at a rate of 50,000 – 100,000 IU per kg of body weight per injection, with an interval of 3-4 days between injections. The 600,000 IU dosage form is used for pediatric dosing.

The duration of treatment is determined by the doctor. Even if the symptoms of the disease disappear quickly, it is necessary to complete the full course of therapy prescribed by the doctor to prevent relapses and the development of microbial resistance.

Adverse Reactions

Adverse reactions are classified by organ systems and frequency. Allergic reactions are the most common. These can range from skin manifestations (maculopapular rash, urticaria, pruritus) to severe, life-threatening conditions such as anaphylactic shock, angioedema (Quincke’s edema), and Stevens-Johnson syndrome. If any signs of allergy appear, the drug should be discontinued immediately and a doctor should be consulted.

From the nervous system: Headache, dizziness, tremor, hyperreflexia, and in high doses (especially in renal failure) – convulsions, signs of neurotoxicity. The so-called Hoigne’s syndrome (acute psychotic reaction, fear of death, auditory and visual disturbances) may occur due to the accidental intravascular entry of the procaine component.

From the digestive system: Nausea, vomiting, diarrhea, glossitis, stomatitis. Pseudomembranous colitis, caused by Clostridium difficile, can develop during or after antibiotic therapy, manifested by severe, persistent diarrhea.

From the blood and lymphatic system: Leukopenia, neutropenia, thrombocytopenia, agranulocytosis, hemolytic anemia, coagulation disorders. With prolonged use, regular monitoring of the peripheral blood picture is necessary.

From the urinary system: Interstitial nephritis, impaired renal function, the appearance of protein and cylinders in the urine.

Local reactions: Pain, induration, and inflammatory reaction at the injection site. With improper technique, damage to the nerve trunk is possible.

Other: Jarisch-Herxheimer reaction (exacerbation of symptoms at the beginning of treatment for syphilis, yaws, and other spirochetal infections due to the mass death of pathogens), superinfection (including fungal).

Drug Interactions

The simultaneous use of Benzycillin-3 with bacteriostatic antibiotics (tetracyclines, macrolides, chloramphenicol, sulfonamides) may lead to a decrease in its bactericidal effect due to the suppression of microbial growth, which is necessary for the manifestation of the action of penicillins.

Probenecid, by competitively blocking tubular secretion, reduces the excretion of benzylpenicillin, which leads to an increase in its concentration in the blood plasma and an increase in the half-life, thereby increasing both the therapeutic effect and the risk of toxic reactions.

Benzycillin-3 may reduce the effectiveness of oral contraceptives. It is recommended to use additional non-hormonal methods of contraception during antibiotic therapy and for one week after its completion.

When used concomitantly with allopurinol, the risk of developing non-allergic skin rashes increases. The drug may potentiate the effect of indirect anticoagulants (by suppressing intestinal microflora that produce vitamin K), which may require dose adjustment of the anticoagulant.

Concomitant use with potassium-sparing diuretics, ACE inhibitors, and angiotensin II receptor antagonists increases the risk of hyperkalemia due to the potassium content in the benzylpenicillin sodium salt. Incompatibility: It is pharmaceutically incompatible with aminoglycosides (mutual inactivation), amphotericin B, ascorbic acid, B vitamins, and some other drugs; they should not be mixed in the same syringe.

Overdose

In case of an overdose of Benzycillin-3, a toxic effect on the central nervous system, including convulsions, encephalopathy, and impaired consciousness, is possible, especially in patients with renal failure or when very high doses are administered. The development of electrolyte imbalances (hyperkalemia, hypernatremia) is also likely due to the potassium and sodium content in the drug salts.

Treatment of overdose is symptomatic and supportive. There is no specific antidote. In case of convulsions, anticonvulsant therapy (diazepam, phenobarbital) is used. In case of severe renal impairment, hemodialysis is effective for removing benzylpenicillin from the bloodstream and correcting electrolyte disturbances. It is necessary to monitor vital functions and the electrolyte composition of the blood.

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.