关键词: 肾移植, 霉酚酸, 药代动力学, 血药浓度监测

Abstract:

ABSTRACT Mycophenolic Acid (MPA) is a metabolite derived from gastro-intestinal absorption of mycophenolate mofetil (MMF) or enteric-coated mycophenolate sodium (EC-MPS) and transforms into MPAG. Pharmacokinetic studies in mass have shown significant inter-patient variability and a time-dependent intra-patient change. It could be influenced by many factors including race, humanity, donor kidney function, serum albumin level, and combined calcineurin inhibitors types. The concentration-effect relationship and significant variability seen in pharmacokinetics of MPA in both inter- and intra-individual are sufficient evidences for MPA therapeutic drug monitoring. The plasma concentration of MPA can be examined in two different methods via high-performance liquid chromatography ( HPLC ) and enzyme immunoassay ( EIA ). For therapeutic drug monitoring of immunosuppressive drugs, its dosage does not feasibly predict the exposure value. MPA-AUC0-12h is observed for its exposure value and is the golden standard for therapeutic drug monitoring. The target range control exposure of MPA-AUC0-12h in the kidney transplant recipients is generally considered between 30 mg.h/L to 60 mg.h/L. Under its lower concentration increases the risk of acute rejection, while above the upper concentration has no apparent additional benefit, but neither drug toxicity associated. Although it is still not conclusive about whether MPA therapeutic drug monitoring is beneficial for patients, but it indeed has brought significant importance for conducting clinical rational drug use of MMF. Summarizing the research progress about therapeutic drug monitoring of mycophenolic acid(MPA) in kidney transplant recipients since last decade, this review underlines the further rational use of MPA and hence explores clues in advanced anti-rejection therapy.

Key words: Kidney transplantation, Mycophenolic acid, Pharmacokinetics, Therapeutic drug monitoring