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机构地区:[1]中国人民解放军南京总医院药理科,南京210002
出 处:《中国临床药理学杂志》2017年第21期2179-2181,共3页The Chinese Journal of Clinical Pharmacology
摘 要:慢性肾衰竭降低药物肾清除率的同时,还会干扰正常的体内代谢过程,多种药物代谢酶、转运体的表达量、活性等均会发生改变。肠道内药物外排减少、代谢降低增加了药物的生物利用度,而肝内摄取转运体减少、外排转运体增多则降低了细胞内药物浓度,并放大代谢酶减少所导致的非肾清除率降低,使得华法林等治疗窗窄的药物出血风险增大。因此,慢性肾衰竭患者除合理调整主要经肾消除药物外,还需关注非肾消除药物的用药剂量。本文对慢性肾衰竭影响药物体内代谢、转运过程进行分析,为临床个体化调整非肾消除药物剂量提供理论基础。Chronic renal failure can reduce the renal clearance rate,as well as interfere with the normal metabolic process. A variety of drug-metabolizing enzymes and transporters are affected by chronic renal failure. The bioavailability increased as the result of more drug efflux and less metabolism in intrauterine,and the non-renal clearance rate decreased as the result of less uptake, more efflux and less metabolism in liver. These changes reduced the safety of drugs with narrow therapeutic window,such as warfarin,in chronic renal failure.Therefore,it is important for chronic renal failure patients to adjust the dose of drugs eliminated by either renal or non-renal reasonably. This paper summarized the changes of drug metabolism and transport induced by chronic renal failure,with the aim to provide a theoretical basis for clinical adjustment of non-renal clearance drugs.
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