Lindholm A
Department of Clinical Pharmacology, Huddinge Hospital, Sweden.
Eur J Clin Pharmacol. 1991;40(6):571-5. doi: 10.1007/BF00279972.
The free fraction of cyclosporine A (CsA) and its total plasma concentration as determined by HPLC(CsAT) were prospectively monitored in 66 recipients of renal transplants. The free CsA levels (CsAu) were calculated. The variability in free CsA levels was no less than for total CsAT levels. The correlation between CsAu and CsAT was high (r = 0.90). Both CsAT and CsAu covaried with serum triglycerides and apolipoprotein A1. Fourty-four of the 66 patients suffered acute rejection episodes on 69 occasions. CsAT and CSAu both decreased and to a similar extent at the occurrence of acute rejection (42% and 59% decrease, respectively; significant vs baseline. Not significant difference in decrease in CsAT vs CsAu). Acute nephrotoxicity occurred on 11 occasions in 10 patients. Both CsAT and CSAu were approximately twice as high at the time of acute nephrotoxicity as compared to one week previously. Both CsAT and CsAu were higher during the first month after transplantation in patients with than in patients without systemic infection. Thus, plasma CsAu gave no additional clinical information or guidance compared to CsAT in renal transplant recipients. Due to the complexity of its assay, which requires two consecutive analyses, there does not appear to be any need for routine monitoring of CsAu in renal transplant recipients.
通过高效液相色谱法（HPLC）测定了66例肾移植受者中环孢素A（CsA）的游离分数及其总血浆浓度（CsAT），并进行前瞻性监测。计算了游离CsA水平（CsAu）。游离CsA水平的变异性不少于总CsAT水平。CsAu与CsAT之间的相关性很高（r = 0.90）。CsAT和CsAu均与血清甘油三酯和载脂蛋白A1共同变化。66例患者中有44例在69次出现急性排斥反应。急性排斥反应发生时，CsAT和CSAu均下降，且下降程度相似（分别下降42%和59%；与基线相比有显著差异。CsAT与CsAu下降幅度无显著差异）。10例患者发生11次急性肾毒性。急性肾毒性发生时，CsAT和CSAu均比一周前高出约两倍。有全身感染的患者移植后第一个月的CsAT和CsAu均高于无全身感染的患者。因此，在肾移植受者中，与CsAT相比，血浆CsAu没有提供额外的临床信息或指导。由于其检测方法复杂，需要连续两次分析，因此肾移植受者似乎没有必要常规监测CsAu。
