Akagi H, Reynolds A, Hjelm M
Institute of Child Health, Hospital for Sick Children, London, UK.
J Int Med Res. 1991 Jan-Feb;19(1):1-18. doi: 10.1177/030006059101900101.
Cyclosporin A (CsA), a non-myelotoxic immunosuppressant, and its metabolites are widely distributed in the body. Highest concentrations of CsA have been detected in the pancreas, adipose tissue and liver, lowest concentrations in brain, muscle, blood and other body fluids. Metabolites are distributed differently to CsA. In addition to lipid partition, intracellular binding to cyclophilin, a peptidyl-prolyl cis-trans isomerase, appears to play a role in its tissue distribution. The temperature dependence of such binding in erythrocytes poses difficulty in serum or plasma measurements. Tissue specific processes may also influence action and toxicity of CsA and its metabolites; thus, a better understanding of the complex distribution pattern of CsA and its metabolites would be important for establishing improved strategies and selection of appropriate specific methodologies for drug monitoring.
环孢素A（CsA）是一种非骨髓毒性免疫抑制剂，其代谢产物在体内广泛分布。CsA在胰腺、脂肪组织和肝脏中的浓度最高，在脑、肌肉、血液和其他体液中的浓度最低。代谢产物的分布与CsA不同。除了脂质分配外，与亲环蛋白（一种肽基脯氨酰顺反异构酶）的细胞内结合似乎在其组织分布中起作用。红细胞中这种结合的温度依赖性给血清或血浆测量带来了困难。组织特异性过程也可能影响CsA及其代谢产物的作用和毒性；因此，更好地了解CsA及其代谢产物的复杂分布模式对于建立改进的策略和选择合适的特定药物监测方法非常重要。
