1. Cefotiam was demonstrated to be more potent than cefazolin in its antibacterial activities against clinical isolates of E. coli, Klebsiella, Serratia, Proteus mirabilis, Proteus morganii and Proteus inconstans. MICs of cefotiam with 10(6) cells/ml inoculum size were considerably lower than those with 10(8) cells/ml. 2. Organisms lysed when exposed to cefotiam at concentrations higher than the MICs with 10(8) cells/ml. Morphological changes of organisms into filament occurred even at concentrations lower than the MICs with 10(6) cells/ml. This indicates that cefotiam is incorporated into organisms at remarkably low concentrations and exerts its antibacterial activities. 3. Cefotiam showed a high affinity for penicillin-binding proteins (PBP) 1A, 1Bs and 3. The formation of filament at low concentrations of cefotiam is possibly attributable to the high affinity of cefotiam for PBP 3 in addition to its high permeability through outer cell membrane. 4. As the antibacterial activities of cefotiam are displayed at lower concentrations, it is reasonable to consider that doses of cefotiam on clinical use can be reduced in comparison with those of conventional cephalosporins.
Cefazolin Enterobacteriaceae