Critically ill patients generally receive moxifloxacin intravenously to achieve rapid bacterial killing. An early switch from intravenous to enteral moxifloxacin may be considered because of its good oral bioavailability in healthy volunteers. Since bioavailability may be altered in critically ill patients due to pathophysiological changes, this study aimed to investigate whether enteral moxifloxacin is bioequivalent to intravenous moxifloxacin in such patients. Blood samples were obtained from 4 critically ill patients before and at serial time-points after intravenous and enteral administration. In all patients, lower maximum plasma concentration (C(max)) and area under the plasma concentration-time curve during the 24-h observation period (AUC(24h)) values were observed after enteral administration compared to those after intravenous administration. This resulted in lower C(max)/minimum inhibitory concentration (MIC) and AUC(24h)/MIC values, which are 2 indices predicting the antibacterial efficacy of moxifloxacin. Despite the limited number of subjects, we conclude that a switch from intravenous to enteral moxifloxacin is not recommended in these patients, because the 2 administration forms are not bioequivalent.