de Smet Julie, Colpaert Kirsten, de Paepe Peter, van Bocxlaer Jan, Decruyenaere Johan, Boussery Koen
Laboratory of Medical Biochemistry and Clinical Analysis, Faculty of Pharmaceutical Sciences, Ghent University, Ghent, Belgium.
Scand J Infect Dis. 2012 Nov;44(11):874-8. doi: 10.3109/00365548.2012.693194. Epub 2012 Jul 17.
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.
重症患者通常静脉注射莫西沙星以实现快速杀菌。鉴于其在健康志愿者中良好的口服生物利用度，可考虑早期从静脉注射莫西沙星转为肠内给予莫西沙星。由于重症患者的病理生理变化可能会改变生物利用度，本研究旨在调查肠内给予莫西沙星在此类患者中是否与静脉注射莫西沙星生物等效。在4例重症患者静脉注射和肠内给予莫西沙星之前及之后的连续时间点采集血样。在所有患者中，与静脉注射后相比，肠内给药后观察到较低的最大血浆浓度（C(max)）和24小时观察期内血浆浓度-时间曲线下面积（AUC(24h)）值。这导致较低的C(max)/最低抑菌浓度（MIC）和AUC(24h)/MIC值，这是预测莫西沙星抗菌疗效的2个指标。尽管受试者数量有限，但我们得出结论，不建议在这些患者中从静脉注射莫西沙星转为肠内给予莫西沙星，因为这两种给药方式并非生物等效。
