Objective:To review current researches on clinical pharmacokinetics and pharmacodynamics of glucocorticoid prednisone/prednisolone in patients receiving renal transplantation in recent years, and to provide references for optimization of immune suppression treatment in the future.Methods: By searching the related literatures worldwide, the current status of related pharmacokinetic/pharmacodynamic researches on prednisone/prednisolone in patients receiving renal transplantation was summarized as well as its future developing direction.Results: Glucocorticoids have been used for many years but their clinical dosing regimens usually depend on physician's experience lacking guidance of pharmacokinetic/pharmacodynamic studies. Thus there are multiple side effects in patients receiving bolus or long-term treatment. At present, clinical pharmacokinetic and pharmacodynamic studies of prednisone/prednisolone in patients receiving renal transplantation have some limitations: the calculation of pharmacokinetic parameters used non-compartmental analysis and two-step statistical methods; in most researches, blood concentrations of total drug concentration are determined rather than free drug concentrations. Pharmacodynamic studies are mostly limited to correlation between drug exposure and toxicity.Conclusion:There have been a few studies on clinical pharmacokinetics and pharmacodynamics of prednisone/prednisolone in patients receiving renal transplantation which are still not comprehensive. Quantitative relationships need to be surveyed to develop guidance of individualized dosage strategies in the future.%目的:综述近年来肾移植术后糖皮质激素泼尼松/泼尼松龙临床药动学(PK)和药效学(PD)研究现状,为进一步优化其免疫抑制治疗方案提供参考.方法:检索国内外相关文献,总结泼尼松/泼尼松龙在肾移植术后药动学/药效学相关研究情况及未来发展方向.结果:糖皮质激素已应用多年,但其临床给药方案通常凭医生经验制定,缺乏临床药动学/药效学研究指导,因而在进行冲击治疗和长期给药时往往出现多种毒副作用.目前泼尼松/泼尼松龙肾移植术后的临床药动学和药效学研究局限:大部分药动学数据采用非房室分析方法以及两步统计法计算,大多数研究中测定血药浓度为总药物浓度而非实际起效的游离药物浓度,药效学研究多限于药物暴露与毒副作用之间的相关性研究.结论:泼尼松/泼尼松龙肾移植术后的临床药动学、药效学研究具有一定基础但尚不全面,有待考察其系统的定量关系用于指导个体化用药方案的制定.
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