Kaplan B, Friedman G, Jacobs M, Viscuso R, Lyman N, DeFranco P, Bonomini L, Mulgaonkar S P
Department of Renal Transplantation, Saint Barnabas Medical Center, Livingston, New Jersey 07039, USA.
Transplantation. 1998 May 27;65(10):1399-400. doi: 10.1097/00007890-199805270-00021.
Troglitazone (Rezulin) is a promising new oral hypoglycemic agent recently approved by the Federal Drug Administration for use in type II diabetes mellitus. Although troglitazone is not metabolized by the cytochrome p450 3A isozyme family, it is a potential inducer of this system. Other medications, e.g., rifampin and phenobarbital, which also induce p450 3A activity, have been reported to significantly decrease cyclosporine (CsA) concentrations.
We report a case of a stable renal transplant patient who had a decrease in CsA concentration after beginning troglitazone and who subsequently developed an acute rejection episode. We then reviewed all stable renal patients begun on troglitazone over the previous 6 months.
The seven transplant patients who had been started on troglitazone therapy experienced a statistically and clinically significant decrease in CsA 12-hr trough levels immediately after the institution of troglitazone therapy.
A potential interaction exists between troglitazone and CsA. Transplant patients on CsA who receive troglitazone therapy should be monitored closely.
曲格列酮（瑞脂宁）是一种有前景的新型口服降糖药，最近已获美国食品药品监督管理局批准用于II型糖尿病的治疗。尽管曲格列酮不由细胞色素P450 3A同工酶家族代谢，但它是该系统的潜在诱导剂。据报道，其他也能诱导P450 3A活性的药物，如利福平及苯巴比妥，可显著降低环孢素（CsA）的浓度。
我们报告了1例肾移植稳定患者，其在开始使用曲格列酮后CsA浓度降低，随后发生急性排斥反应。然后，我们回顾了过去6个月内开始使用曲格列酮的所有稳定肾移植患者。
接受曲格列酮治疗的7例移植患者在开始使用曲格列酮治疗后，CsA的12小时谷浓度立即出现了具有统计学意义和临床意义的下降。
曲格列酮与CsA之间可能存在相互作用。接受曲格列酮治疗的服用CsA的移植患者应密切监测。
