title: In vitro antibacterial properties of cefetamet and in vivo activity of its orally absorbable ester derivative, cefetamet pivoxil.
abstract: The in vitro activity of cefetamet, the microbiologically active metabolite of the orally administered prodrug cefetamet pivoxil, was compared with that of cephalexin, cefaclor, cefuroxime and amoxicillin. Cefetamet was highly active against Enterobacteriaceae, Neisseria spp., Vibrio spp., Haemophilus influenzae and streptococci other than enterococci. Cefetamet inhibited cefaclor-resistant species such as Proteus vulgaris, Providencia stuartii, Providencia rettgeri and Serratia marcescens. Staphylococci, Pseudomonas aeruginosa and cephalosporinase-overproducing strains of Enterobacter cloacae were resistant to cefetamet. The superior activity of cefetamet compared with older oral beta-lactam antibiotics against a large number of gram-negative pathogens correlated with enhanced stability towards beta-lactamases. In accordance with the in vitro findings, cefetamet pivoxil showed good activity in experimental infections in the mouse and rat, suggesting satisfactory bioavailability in these animals after oral administration.
authors.affiliation: Pharmaceutical Research, F. Hoffmann-La Roche & Co., Basel, Switzerland.
authors.forename: P
authors.initials: P
authors.lastname: Angehrn
authors.forename: P
authors.initials: P
authors.lastname: Hohl
authors.forename: R L
authors.initials: RL
authors.lastname: Then
mesh_terms: D000818:Animals; D001419:Bacteria / Q000187:drug effects*; D001426:Bacterial Proteins; D002352:Carrier Proteins / Q000378:metabolism; D015296:Ceftizoxime / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology / Q000627:therapeutic use; D004352:Drug Resistance, Microbial; D004755:Enterobacteriaceae / Q000187:drug effects*; D006193:Haemophilus influenzae / Q000187:drug effects; D006602:Hexosyltransferases; D006801:Humans; D051379:Mice; D008826:Microbial Sensitivity Tests; D002267:Muramoylpentapeptide Carboxypeptidase / Q000378:metabolism; D009343:Neisseria / Q000187:drug effects; D046915:Penicillin-Binding Proteins; D010458:Peptidyl Transferases; D051381:Rats; D018805:Sepsis / Q000188:drug therapy*; D013291:Streptococcus / Q000187:drug effects; D014733:Vibrio / Q000187:drug effects; D001618:beta-Lactamases / Q000378:metabolism
chemical_list: D001426:Bacterial Proteins; D002352:Carrier Proteins; D046915:Penicillin-Binding Proteins; C047444:cefetamet; D015296:Ceftizoxime; D010458:Peptidyl Transferases; D006602:Hexosyltransferases; D002267:Muramoylpentapeptide Carboxypeptidase; D001618:beta-Lactamases; C047445:cefetamet pivoxyl