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Procaine Benzylpenicillin – Uses, Dosage, Side Effects

Procaine benzylpenicillin is a depot antibiotic from the penicillin group, administered by injection, which allows for a slow and sustained release of the active substance.

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Things worth knowing about "Procaine Benzylpenicillin"

Procaine benzylpenicillin is a depot antibiotic from the penicillin group, administered by injection, which allows for a slow and sustained release of the active substance.

What is Procaine Benzylpenicillin?

Procaine benzylpenicillin (also known as procaine penicillin) is an antibiotic belonging to the beta-lactam class. It is a salt compound formed from benzylpenicillin (Penicillin G) and the local anaesthetic procaine. This combination creates a depot formulation: after intramuscular injection, the active ingredient is released slowly from the muscle tissue, providing a prolonged therapeutic level in the bloodstream.

Indications

Procaine benzylpenicillin is used to treat various bacterial infections caused by penicillin-susceptible organisms:

Syphilis – one of the primary indications, including early and late-stage disease
Pneumonia caused by Streptococcus pneumoniae
Streptococcal infections of the throat and skin
Erysipelas (skin infection caused by streptococci)
Anthrax (post-exposure prophylaxis and treatment)
Other infections caused by gram-positive bacteria and spirochaetes

Mechanism of Action

Benzylpenicillin works by inhibiting bacterial cell wall synthesis. It binds to penicillin-binding proteins (PBPs) – enzymes responsible for building and maintaining the structural integrity of the bacterial cell wall. When these proteins are blocked, the cell wall weakens and the bacteria can no longer survive. The procaine component acts solely as a carrier substance to slow absorption, creating the depot effect – it has no antibacterial activity of its own.

Dosage and Administration

Procaine benzylpenicillin is administered exclusively as an intramuscular (IM) injection. Intravenous administration is absolutely contraindicated due to the risk of severe adverse reactions. Dosage is determined by the treating physician based on the indication, body weight, and clinical condition.

Early syphilis: Typically 600,000–1,200,000 IU daily for several days
Late syphilis / neurosyphilis: Often 2,400,000 IU daily for 10–14 days
Always follow the dosage instructions provided by a healthcare professional

Side Effects

Like all antibiotics, procaine benzylpenicillin may cause side effects. The most common include:

Allergic reactions: Ranging from skin rash to severe anaphylaxis (rare)
Procaine toxicity: Dizziness, tinnitus, tingling sensations, anxiety, confusion, or brief loss of consciousness – particularly if the injection is accidentally given into a blood vessel
Hoigne syndrome: Transient psychological reactions such as anxiety, hallucinations, or confusion due to procaine
Pain and swelling at the injection site
Gastrointestinal discomfort (uncommon)

Contraindications and Warnings

Procaine benzylpenicillin should not be used in patients with:

Known hypersensitivity to penicillins or cephalosporins (cross-reactivity possible)
Known allergy to procaine or other ester-type local anaesthetics
Intravenous administration – absolutely contraindicated

A thorough allergy history should always be taken before use. Emergency resuscitation facilities should be available at the time of first administration.

Drug Interactions

Certain medications may interact with procaine benzylpenicillin:

Probenecid reduces the renal excretion of penicillin, increasing blood levels and prolonging the effect
Bacteriostatic antibiotics (e.g., tetracyclines, chloramphenicol) may reduce the efficacy of penicillins
Oral contraceptives: A potential reduction in effectiveness has been reported in rare cases

References

World Health Organization (WHO): Model Formulary 2008 – Antibacterials. Geneva: WHO Press, 2008.
Mutschler E. et al.: Mutschler Drug Effects – Pharmacology, Clinical Pharmacology, Toxicology. 11th edition. Stuttgart: Wissenschaftliche Verlagsgesellschaft, 2020.
European Centre for Disease Prevention and Control (ECDC): Sexually Transmitted Infections in Europe – Management Guidelines, including Syphilis Treatment. Stockholm: ECDC, 2023.

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