Yanagimoto Hiromi, Teramatsu Tsuyoshi, Goto Junko, Yanagisawa Masahiko, Harii Norikazu, Suzuki Masahiko, Hanawa Takehisa, Matsuda Kenichi, Oguchi Toshio
Department of Pharmacy, University Hospital, University of Yamanashi, 1110 Shimokato, Chuo, Yamanashi 409-3898, Japan.
Yakugaku Zasshi. 2013;133(6):711-7. doi: 10.1248/yakushi.13-00002. Epub 2013 Apr 5.
Variation in protein binding ratio (PBR) of teicoplanin (TEIC) was investigated in continuous hemodiafiltration (CHDF) patients. TEIC is classified as a high PBR drug (≧90%), and it was reported that the PBR of TEIC decreased with an decrease in the serum albumin level in hypoalbuminemia patients. However, few reports can be found about the variation of PBR of TEIC for CHDF patient. An antibiotic activity is directly determined by the level of unbound antibiotics species (Cfree) in the target site, namely, an increase in the Cfree enhances the risks of TEIC as well as the therapeutic effect against Methicillin-resistant Staphylococcus aureus (MRSA). In this study, both the total concentration (Ctotal) and Cfree of TEIC were determined and the PBRs were compared between a patient with normal albumin level, hypoalbuminemia patients and CHDF patients. Similarly to the previous report, the lowering of PBR of TEIC was demonstrated in the hypoalbuminemia patients. On the other hand, the CHDF patients showed lower value of PBR suggesting some change in the protein binding ability, although showed higher values of serum albumin level in comparison with the hypoalbuminemia patients. It was not necessary to measure the Cfree value for the hypoalbuminemia patient routinely, but the monitoring of Cfree as well as Ctotal for the CHDF patients can be important for the proper TEIC use because of the potential specialty of PBR.
在连续性血液透析滤过（CHDF）患者中研究了替考拉宁（TEIC）的蛋白结合率（PBR）变化。TEIC被归类为高蛋白结合率药物（≧90%），据报道，在低白蛋白血症患者中，TEIC的PBR随血清白蛋白水平降低而下降。然而，关于CHDF患者TEIC的PBR变化的报道很少。抗生素活性直接由靶部位未结合抗生素种类的水平（Cfree）决定，即Cfree升高会增加TEIC的风险以及对耐甲氧西林金黄色葡萄球菌（MRSA）的治疗效果。在本研究中，测定了TEIC的总浓度（Ctotal）和Cfree，并比较了白蛋白水平正常的患者、低白蛋白血症患者和CHDF患者之间的PBR。与之前的报道相似，低白蛋白血症患者中TEIC的PBR降低。另一方面，CHDF患者的PBR值较低，表明蛋白结合能力有一些变化，尽管与低白蛋白血症患者相比血清白蛋白水平较高。对于低白蛋白血症患者，常规测量Cfree值没有必要，但由于PBR的潜在特殊性，监测CHDF患者的Cfree以及Ctotal对于正确使用TEIC可能很重要。
