The therapeutic use of oral cephalosporins to treat infectious diseases con
tinues to challenge clinicians; many attempts have been made over recent ye
ars to improve the efficacy and spectrum of these anti-infectives. Many ora
l cephalosporins are in development and include cefdinir, cefprozil, cefeta
met pivoxil, cefcapene pivoxil, cefcanel daloxate hydrochloride in Phase II
trials, S-1090 in Phase III trials and the novel compounds E1100, E1101 an
d BRL-57347. Differences between these drugs are sometimes subtle and the i
mprovement over existing compounds modest, although recent cephalosporins h
ave shown greater activity against Gram-negative bacterial infections. A be
tter knowledge of the pharmacodynamic and pharmacokinetic interrelationship
s of existing oral cephalosporins is demanded for a more rational use of th
ese compounds and to avoid the subsequent development of resistance. Perhap
s with such an approach, the perceived need for new cephalosporins will dim
inish.