Scaglione F
Department of Pharmacology, University of Milan, Italy.
Pediatr Infect Dis J. 1997 Mar;16(3 Suppl):S56-9. doi: 10.1097/00006454-199703001-00006.
Both the in vitro microbiologic activity of an antibiotic drug and its pharmacokinetic characteristics are important criteria to be considered when predicting clinical efficacy. At present, however, it is not clear which pharmacokinetic parameters are the most useful in determining optimal therapeutic approaches.
To review the various pharmacokinetic properties of antibiotics, with special reference to the cephalosporins, and to consider the contributions that these make to the definitive prediction of clinical efficacy.
It is important, when attempting to use the pharmacokinetic parameters in conjunction with the minimum inhibitory concentrations for possible pathogens to predict clinical efficacy, to measure the concentration of an antibacterial drug at the site of bacterial proliferation. In most cases bacteria proliferate in the interstitial fluid; therefore it is important to choose an antibiotic that achieves high concentrations in this compartment; the intracellular concentration is less critical. The interstitial fluid concentration is in equilibrium with the free (i.e. non-protein-bound) serum concentration and either of these antibiotic levels is more predictive of clinical efficacy than are intracellular levels.
在预测临床疗效时，抗生素药物的体外微生物活性及其药代动力学特征都是需要考虑的重要标准。然而目前尚不清楚哪些药代动力学参数在确定最佳治疗方法时最为有用。
综述抗生素的各种药代动力学特性，特别提及头孢菌素类，并考量这些特性对临床疗效最终预测的贡献。
在试图结合可能病原体的最低抑菌浓度使用药代动力学参数来预测临床疗效时，测量抗菌药物在细菌增殖部位的浓度很重要。在大多数情况下，细菌在组织间液中增殖；因此选择一种能在该腔隙中达到高浓度的抗生素很重要；细胞内浓度的重要性较低。组织间液浓度与游离（即非蛋白结合）血清浓度处于平衡状态，这些抗生素水平中的任何一个都比细胞内水平更能预测临床疗效。
