Antibiotic therapy is constantly changing. Among the criteria used to
choose the right antibiotic, tissue pharmacokinetics provides useful,
though controversial, information on drug distribution in organs and b
ody fluids at potential sites of infection. Various study models have
established i) the high rate of penetration of third-generation cephal
osporins, aminoglycosides and fluoroquinolones into cerebrospinal flui
d when meninges are inflamed; and ii) high levels of macrolides and fl
uoroquinolones in lung parenchyma and other respiratory sites of infec
tion. These data should be analyzed in terms of pharmacodynamic activi
ties in sites in the cerebrospinal fluid where the minimum inhibitory
concentration and the minimum bactericidal concentration have been det
ermined for the pathogen, In other situations, the criteria with the m
ost clinical significance is the correlation between tissue concentrat
ions and clinical outcome. There has been much progress in targeted (l
iposomes) antibiotic therapy with promising advances toward better tis
sue distribution of drugs.