Xu L, Cai M, Shi B-Y, Li Z-L, Li X, Jin H-L
Transplantation Institutes, The 309th Hospital of the Chinese PLA, Beijing, China.
Transplantation Institutes, The 309th Hospital of the Chinese PLA, Beijing, China.
Transplant Proc. 2014 Jun;46(5):1362-5. doi: 10.1016/j.transproceed.2014.01.012.
Enteric-coated mycophenolate sodium (EC-MPS) and mycophenolate mofetil (MMF), two prodrugs of mycophenolic acid (MPA), have been used in immunosuppressive regimens. After being taken orally, both of them transform to MPA to achieve immune suppression effects; however, the main site of absorption and metabolism of EC-MPS is different from that of MMF in vivo. Therefore, combined application with related drugs may result in different MPA levels and have different clinical effects in kidney transplant recipients.
To evaluate the efficacy of EC-MPS compared with MMF in Chinese renal transplant patients comedicated with a proton pump inhibitor (PPI).
Our subjects were 88 patients who received renal transplants at the 309th Hospital of the Chinese PLA from May 2010 to April 2013. These were made up of two groups including 27 patients with EC-MPS and 61 with MMF. The immunosuppression regimen was EC-MPS/MMF + cyclosporine/tacrolimus + steroid hormone, comedicated with a PPI (omeprazole). The patients' levels of exposure of MPA within 1 week after operation were monitored. Clinical indicators such as incidence of delayed graft function and acute rejection, the rate of change of serum creatinine hemoglobin, leucocytes, and neutrophils, as well as clinical adverse drug reactions and drug conversion were analyzed retrospectively.
The kidney function of patients recovered to normal in both the EC-MPS and MMF groups. The mean concentration to peak (Cmax), the mean half-life (t1/2), and the area under the concentration-time curve (AUC0-12) of MPA in the EC-MPS group were higher than those in the MMF group (P < .05). This indicated that the pharmacokinetic parameters for MPA when EC-MPS is co-administered with a PPI in kidney transplant patients in China is better than for comedication with MMF and a PPI. The MMF group had a higher incidence of drug withdrawal because of higher infection rates, leucocyte decrease, and more gastrointestinal side effects than the EC-MPS group (P < .05). No significant differences in the clinical effect on kidney transplant recipients were observed in the limited observation time.
肠溶包衣的麦考酚钠（EC-MPS）和霉酚酸酯（MMF）是霉酚酸（MPA）的两种前体药物，已用于免疫抑制方案。口服后，它们都会转化为MPA以实现免疫抑制作用；然而，EC-MPS在体内的主要吸收和代谢部位与MMF不同。因此，与相关药物联合应用可能导致MPA水平不同，并在肾移植受者中产生不同的临床效果。
在中国肾移植患者中，评估与MMF相比，EC-MPS与质子泵抑制剂（PPI）联合应用的疗效。
我们的研究对象为2010年5月至2013年4月在中国人民解放军第309医院接受肾移植的88例患者。这些患者分为两组，其中27例使用EC-MPS，61例使用MMF。免疫抑制方案为EC-MPS/MMF + 环孢素/他克莫司 + 类固醇激素，并联合使用PPI（奥美拉唑）。监测患者术后1周内MPA的暴露水平。回顾性分析临床指标，如移植肾功能延迟恢复和急性排斥反应的发生率、血清肌酐、血红蛋白、白细胞和中性粒细胞的变化率，以及临床药物不良反应和药物转换情况。
EC-MPS组和MMF组患者的肾功能均恢复正常。EC-MPS组MPA的平均达峰浓度（Cmax）、平均半衰期（t1/2）和浓度-时间曲线下面积（AUC0-12）均高于MMF组（P <.05）。这表明在中国肾移植患者中，EC-MPS与PPI联合应用时MPA的药代动力学参数优于MMF与PPI联合应用。由于感染率较高、白细胞减少以及胃肠道副作用较多，MMF组因药物停用的发生率高于EC-MPS组（P <.05）。在有限的观察时间内，未观察到对肾移植受者临床效果的显著差异。
