Effective antibiotic treatment of critically ill patients remains a significant challenge to intensivists world-wide with persisting high mortality and morbidity rates. Pathophysiological changes in critically ill patients lead to changes in the pharmacokinetics (PK)/pharmacodynamics (PD) of antibiotics. Optimizing the current antibiotic delivery regimen is an important strategy to cope with this problem. In this paper, we review the PD characteristics and the potential changes of PK of antibiotics in critically ill patients, and the application and research progress of PK/PD in the optimization of antibiotic treatment regimens for them.