Jones T E
Pharmacy Department, Queen Elizabeth Hospital, Woodville South, Australia.
Clin Pharmacokinet. 1997 May;32(5):357-67. doi: 10.2165/00003088-199732050-00002.
Since its discovery in 1970, and introduction into clinical practice in 1978, cyclosporin has become the most important immunosuppressive drug used to prevent organ transplant rejection. This has been achieved by virtue of the improved graft survival rates and adverse effect profiles in patients when compared with that of the older agents. Cyclosporin is substantially more expensive (both to provide and to monitor) however, and the magnitude of these costs may preclude its use, particularly where the transplant recipient is required to pay. Cyclosporin has a complex pharmacokinetic profile with poor absorption, extensive metabolism to more than 30 metabolites and considerable inter- and intrapatient variability. Many transplant centres routinely use drugs ("cyclosporin-sparing agents') to allow a reduction in the dosage of cyclosporin while maintaining therapeutic blood cyclosporin concentrations. The use of a second drug to affect the pharmacokinetic profile of a primary drug is not new, but the use of cyclosporin-sparing agents is a departure from previous practices in that this coprescription is primarily for economic reasons. The decision to use these agents (and the choice of agent) is based upon economic and other factors including the extent of the cyclosporin-sparing effect, the potential for additional therapeutic benefit and/or adverse effects. The coprescription of cyclosporin-sparing agents is ethically more acceptable where the transplant recipient is the economic beneficiary but where the savings accrue to a third party it is more difficult. Benefits to the community at large must be balanced against the risk of adverse effects to the patient. The use of cyclosporin-sparing agents may reduce compliance and hence, jeopardise transplant and/or recipient outcomes. The transplant recipient must be informed about the reasons for their use and advised to consult an experienced physician or pharmacist before altering the established drug regimen.
自1970年被发现并于1978年引入临床实践以来,环孢素已成为预防器官移植排斥反应最重要的免疫抑制药物。与旧的药物相比,这是通过提高患者的移植存活率和改善不良反应情况来实现的。然而,环孢素的成本要高得多(包括供应和监测方面),这些成本的规模可能会妨碍其使用,特别是在移植受者需要自行支付费用的情况下。环孢素具有复杂的药代动力学特征,吸收不良,广泛代谢为30多种代谢物,患者之间和患者自身的变异性都很大。许多移植中心常规使用药物(“环孢素节省剂”),以便在维持治疗性血环孢素浓度的同时减少环孢素的剂量。使用第二种药物来影响主要药物的药代动力学特征并非新鲜事,但使用环孢素节省剂与以往的做法不同,因为这种联合处方主要是出于经济原因。使用这些药物的决定(以及药物的选择)基于经济和其他因素,包括环孢素节省效果的程度、额外治疗益处和/或不良反应的可能性。在移植受者是经济受益者的情况下,联合使用环孢素节省剂在伦理上更容易被接受,但如果节省的费用归第三方所有,则会更加困难。必须在对广大社区的益处与对患者产生不良反应的风险之间进行权衡。使用环孢素节省剂可能会降低依从性,从而危及移植和/或受者的预后。必须告知移植受者使用这些药物的原因,并建议他们在改变既定的药物治疗方案之前咨询经验丰富的医生或药剂师。