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舍曲林的血液透析性。

Hemodialyzability of sertraline.

作者信息

Schwenk M H, Verga M A, Wagner J D

机构信息

St. John's University, College of Pharmacy and Allied Health Professions, Department of Clinical Pharmacy Practice, Jamaica, New York 11439, USA.

出版信息

Clin Nephrol. 1995 Aug;44(2):121-4.

PMID:8529300
Abstract

Sertraline is an antidepressant which selectively inhibits the neuronal uptake of serotonin in the central nervous system. The pharmacokinetics of sertraline in end-stage renal disease (ESRD) and the effect of hemodialysis on sertraline clearance is unknown. A dose of 100 mg sertraline was administered to two anuric hemodialysis patients after hemodialysis. During the next hemodialysis session, simultaneous pre- and post dialyzer blood samples were obtained at the start of and hourly throughout dialysis until completion. All spent dialysate was collected hourly, quantified and an aliquot retained. Additional blood samples were obtained approximately 20 hours after dialysis and prior to the next treatment. Serum and dialysate were assayed for sertraline by gas chromatography-mass spectroscopy. Initial sertraline serum concentrations were similar to those observed in subjects with normal renal function given the same sertraline dose, implying unaltered absorption and distribution. Sertraline was not detected in any dialysate sample. The elimination half-life was 42-92 h (normally 24-36 h), suggesting impaired clearance. Smaller doses of sertraline may be required in ESRD patients, yet post-hemodialysis supplementation is unnecessary.

摘要

舍曲林是一种抗抑郁药,它能选择性抑制中枢神经系统中血清素的神经元摄取。舍曲林在终末期肾病(ESRD)患者中的药代动力学以及血液透析对舍曲林清除率的影响尚不清楚。在血液透析后,给两名无尿的血液透析患者服用了100毫克舍曲林。在下一次血液透析过程中,在透析开始时以及透析全程每小时采集透析器前后的同步血样,直至透析结束。每小时收集所有用过的透析液,进行定量并保留一份等分试样。在透析后约20小时以及下次治疗前采集额外的血样。通过气相色谱 - 质谱法测定血清和透析液中的舍曲林。初始舍曲林血清浓度与给予相同舍曲林剂量的肾功能正常受试者中观察到的浓度相似,这意味着吸收和分布未改变。在任何透析液样本中均未检测到舍曲林。消除半衰期为42 - 92小时(正常为24 - 36小时),表明清除受损。ESRD患者可能需要较小剂量的舍曲林,但血液透析后无需补充。

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