Diez Ojea B, Alonso Alvarez M, Aguado Fernández S, Baños Gallardo M, García Melendreras S, Gómez Huertas E
Hospital Valle del Nalón, Langreo, Spain.
Transplant Proc. 2009 Jul-Aug;41(6):2323-5. doi: 10.1016/j.transproceed.2009.06.048.
MR-4, the new oral formulation of tacrolimus that allows once-daily dosing, may improve patient compliance. The purpose of this study was to evaluate the safety and efficacy parameters among a group of stable renal allografts after conversion to MR-4.
We enrolled 82 stable kidney recipients, who had received their grafts 43.9 +/- 38.3 months prior. They were of mean age 56 +/- 12 years and included 70.7% men. Sixty-six patients were converted on a milligram-for-milligram basis from their total daily dose; the remaining patients were converted at the physician's discretion. Three patients were excluded: 1 because of the development of abdominal pain, and 2 because of dosing errors. Tacrolimus trough levels and renal function tests were evaluated at entry and on days 7, 30, and 90.
Only 5 (7.6%) converted patients required a later dose adjustment. In the group of 61 patients who did not require this adjustment, the mean tacrolimus trough levels decreased during the first week (6.8 +/- 1.7 to 5.8 +/- 2.0; P < .000). Thirty-eight patients completed 3 months of follow-up. Their tacrolimus trough levels, serum creatinine levels, and proteinuria remained stable. The number of capsules per patient needed after the conversion to MR-4 was lower (3.9 +/- 1.6 versus 2.9 +/- 1.0; P < .000). There were no cases of acute rejection episodes.
Based on a milligram-for-milligram conversion, only 7.6% of our patients required a dose adjustment. With this conversion, an initial decrease in tacrolimus trough levels was documented at day 7, which remained stable to the end of the study. The patients needed a lower number of capsules. These results supported the safety of MR-4.
他克莫司新的口服制剂MR-4允许每日一次给药，可能会提高患者的依从性。本研究的目的是评估一组稳定肾移植受者转换为MR-4后的安全性和有效性参数。
我们纳入了82名稳定的肾移植受者，他们在43.9±38.3个月前接受了移植。他们的平均年龄为56±12岁，男性占70.7%。66名患者根据每日总剂量按毫克对毫克的比例进行转换；其余患者由医生酌情转换。三名患者被排除：1名因出现腹痛，2名因给药错误。在入组时以及第7、30和90天评估他克莫司谷浓度和肾功能测试。
只有5名（7.6%）转换患者需要后期调整剂量。在61名不需要这种调整的患者组中，他克莫司谷浓度在第一周下降（6.8±1.7降至5.8±2.0；P<0.000）。38名患者完成了3个月的随访。他们的他克莫司谷浓度、血清肌酐水平和蛋白尿保持稳定。转换为MR-4后每位患者所需的胶囊数量更低（3.9±1.6对2.9±1.0；P<0.000）。没有急性排斥反应事件发生。
基于毫克对毫克的转换，我们只有7.6%的患者需要调整剂量。通过这种转换，第7天记录到他克莫司谷浓度最初下降，到研究结束时保持稳定。患者需要的胶囊数量更少。这些结果支持了MR-4的安全性。
