Cefazolin: A Comprehensive Monograph

I. Executive Summary

Cefazolin is a parenteral, first-generation cephalosporin antibiotic that has served as a workhorse agent in clinical medicine for decades. It functions as a bactericidal agent by irreversibly inhibiting bacterial cell wall synthesis, leading to cell lysis and death. Its primary utility lies in the treatment of infections caused by susceptible Gram-positive cocci, most notably methicillin-susceptible Staphylococcus aureus (MSSA) and Streptococcus species, as well as certain clinically relevant Gram-negative pathogens such as Escherichia coli and Klebsiella pneumoniae. Cefazolin's most prominent role is as the drug of choice for surgical prophylaxis across a vast array of procedures, a status earned through its ideal antimicrobial spectrum, established efficacy, and low cost.

Recent clinical evidence has highlighted a significant paradigm shift in the management of serious MSSA infections, such as bacteremia. Comparative studies consistently demonstrate that Cefazolin possesses a more favorable safety profile than traditional antistaphylococcal penicillins (e.g., nafcillin, oxacillin), with a markedly lower incidence of nephrotoxicity and hepatotoxicity. This superior safety, combined with less frequent dosing requirements and lower cost, increasingly positions Cefazolin as a preferred first-line agent for these infections.