Cefotaxime is a bactericidal agent that exerts its mechanism of action by binding

penicillin-binding proteins (PBPs) via beta-lactam rings and inhibiting the

definitive activity of transpeptidation in peptidoglycan cell wall synthesis of
susceptible bacterial organisms.[8][9] Its action demonstrates a great affinity for
PBP Ib and PBP III cell wall proteins.

The inability to form a bacterial cell wall further causes the autolysis of the
bacteria.[7] Similarly to other third-generation cephalosporins, its broad spectrum
action makes it efficacious against gram-positive and gram-negative bacteria.

Resistance

Beta-lactamases can cause hydrolysis to cefotaxime, further hindering its

bactericidal effects. Although susceptive, cefotaxime is quite durable against the
activity of most β-lactamases.

Metabolism

Once administered, cefotaxime undergoes metabolism within the liver, and the
majority of it is excreted renally. In the liver, cefotaxime converts to
desacetylcefotaxime, which is further converted to desacetylcefotaxime lactone and
then to M metabolites.[10] More than 80% is recovered in the urine, with one-third
being in the form of desacetylcefotaxime (des-CTX). Although desacetylcefotaxime
(des-CTX) is the major metabolite of cefotaxime, its activity is eight-fold weaker
than cefotaxime.[11]