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西替贝纳在慢性肾功能损害中的药代动力学。

Pharmacokinetics of Cytembena in chronic renal impairment.

作者信息

Schück O, Grafnetterová J, Sotorník I

出版信息

Neoplasma. 1976;23(2):161-70.

PMID:947088
Abstract

Renal excretion of Cytembena in subjects with a normal renal function amounted on the average to 7.8% of the given dose during 15 hours following a single intravenous administration of 200 mg of this cytostatic drug. In patients with an impaired renal function there was a further decrease in the urinary Cytembena excretion and this in direct relation to the decrease in endogenous creatinine clearance rate. The decline in renal Cytembena clearance is slower than that of glomerular filtration rate due, probably, to a lowered tubular reabsorption of Cytembena in residual nephrons. This change in tubular resorption of Cytembena is related to a decrease of the fractional reabsorption of sodium in residual nephrons. Serum Cytembena concentrations proved to be significantly lower in patients with impaired renal functions than in subjects with normal renal functions. This peculiarity of the pharmacokinetics of Cytembena is discussed from the aspect of a possible increase of its distribution volume in consequence of an increased concentration of the diffusible component.

摘要

在单次静脉注射200毫克这种细胞抑制药物后的15小时内,肾功能正常的受试者中,塞替派的肾脏排泄量平均占给药剂量的7.8%。在肾功能受损的患者中,尿液中塞替派的排泄量进一步减少,且这与内源性肌酐清除率的降低直接相关。肾脏对塞替派的清除率下降速度比肾小球滤过率慢,这可能是由于残余肾单位中塞替派的肾小管重吸收降低所致。塞替派肾小管重吸收的这种变化与残余肾单位中钠的分数重吸收减少有关。肾功能受损患者的血清塞替派浓度被证明显著低于肾功能正常的受试者。从由于可扩散成分浓度增加导致其分布容积可能增加的方面讨论了塞替派药代动力学的这一特性。

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