An approach to minimization of toxicity of a new compound is to elucid
ate the mechanisms of toxicity of analogous compounds and to clarify t
heir structure-toxicity relationships. A problem with this approach, h
owever, is that such elucidation remains difficult. For quinolones, so
me improvements in this mechanistic approach have been achieved in the
central nervous system (CNS), particularly with regard to their inter
action with nonsteroidal anti-inflammatory drugs (NSAIDs), and in geno
toxicity and phototoxicity studies, particularly in comparison with ot
her toxicities, such as to the cardiovascular, gastrointestinal, bone,
reproductive, and developmental systems. This review concentrates on
a description of the known effects of quinolones on various organ syst
ems in experimental animals and humans. Given the logarithmic increase
in the synthesis of new quinolones, it is questionable whether these
drugs share similar safety and efficacy. Nevertheless, this mechanisti
c approach to the investigation and minimization of toxicity has produ
ced satisfactory results to date and deserves to be continued.