REVIEW Benzathine benzylpenicillin is a form of penicillin antibacterial also known as benzathine penicillin. It is slowly absorbed into the circulation after intramuscular injection and hydrolysed to benzylpenicillin in vivo. It is the drug-of-choice when prolonged low concentrations of benzylpenicillin are required and appropriate, allowing prolonged antibiotic action over 2-4 weeks after a single IM dose. Specific indications for benzathine penicillin include prophylaxis of rheumatic fever and early or latent syphilis. The benzylpenicillin inhibits bacterial cell wall synthesis by binding to one or more of the penicillin-binding proteins (PBPs). This inhibits the final transpeptidation step of peptidoglycan synthesis in bacterial cell walls, thus inhibiting cell wall biosynthesis. Bacteria eventually lyse due to ongoing activity of cell wall autolytic enzymes (autolysins and murein hydrolases) while cell wall assembly is arrested.
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