Kyriakides G, Miller J
The Paraskevaidion Transplant Center of Cyprus, Nicosia, Cyprus.
Transplant Proc. 2004 Mar;36(2 Suppl):167S-172S. doi: 10.1016/j.transproceed.2004.01.112.
Since 1983, cyclosporine has been the backbone of immunosuppression in clinical organ transplantation. Cyclosporine is usually used in combination with steroids and with another second-line immunosuppressant like azathioprine or mycofenolate mofetil. With these regimens, graft survival at 1 year exceeds 90% and long-term results are excellent. The main complication is renal toxicity, which is usually secondary to excessive exposure. The new microemulsion formulation of cyclosporine, introduced in recent years, has improved intestinal absorption and bioavailability and resulted in much less intrapatient variation than the older formulation. The introduction of 2-hour peak blood level monitoring, which corresponds closely to the area under the curve of the drug, allows more appropriate dosing, thus minimizing rejection owing to underexposure or toxicity owing to overexposure. As new effective immunosuppressants are currently becoming available for use in combination with cyclosporine, the transplant community can look forward to more effective and safer immunosuppression.
自1983年以来，环孢素一直是临床器官移植中免疫抑制的核心药物。环孢素通常与类固醇以及另一种二线免疫抑制剂（如硫唑嘌呤或霉酚酸酯）联合使用。采用这些方案，1年时移植物存活率超过90%，长期效果良好。主要并发症是肾毒性，通常继发于药物过度暴露。近年来推出的环孢素新型微乳剂配方改善了肠道吸收和生物利用度，与旧配方相比，患者体内的差异小得多。引入2小时血药峰浓度监测，该监测与药物曲线下面积密切相关，可实现更合理的给药，从而将因暴露不足导致的排斥反应或因暴露过度导致的毒性降至最低。由于目前有新的有效免疫抑制剂可与环孢素联合使用，移植界有望实现更有效、更安全的免疫抑制。
