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硼卡钠对大鼠及脑肿瘤患者的利尿作用。

The diuretic effect of borocaptate sodium in rats and in patients with brain tumors.

作者信息

Horn V, Slánsky J, Buchar E, Janku I, Sourek K, Tovarys F

机构信息

Institute of Pharmacology, Academy of Sciences, Prague, Czech Republic.

出版信息

Methods Find Exp Clin Pharmacol. 1997 Oct;19(8):559-66.

PMID:9442480
Abstract

Kidney function changes after single-dose administration of borocaptate sodium were studied in rats and in patients with brain tumors. Changes of glomerular filtration rate (GFR) measured as 14C-inulin clearance and urine flow rate (UFR) after a slow intravenous injection of BSH (25 and 50 mg/kg b.w., respectively) were investigated in rats under pentobarbital anesthesia. The effect of BSH has been compared with that of its disulfide (BSSB) which is spontaneously generated by oxidation of BSH during storage. It was found that BSH decreases GFR in relation to dose and, in the same way, causes a temporary increase of UFR. On the other hand, BSSB (50 mg/kg) induced a large reversible decrease of GFR as well as a decrease of urine excretion. Measurements of GFR (inulin clearance), renal plasma flow (PAH clearance) and urine excretion were taken in a group of patients with brain tumors in which boron disposition after an infusion of BSH (25 mg/kg b.w. over 1 h) had been studied. An increase in urine production was the dominant effect (up to 200% of the initial value), with the alterations of GFR and RPF being of minor significance except in one patient with a GFR reduction up to almost 50% the original value. Kidney function changes after BSH or BSSB administration are supposedly related to the high retention of BSH in kidney.

摘要

在大鼠和脑肿瘤患者中研究了单次给药硼卡醇钠后的肾功能变化。在戊巴比妥麻醉下,对大鼠缓慢静脉注射硼卡醇钠(分别为25和50mg/kg体重)后,以14C-菊粉清除率测量的肾小球滤过率(GFR)和尿流率(UFR)的变化进行了研究。将硼卡醇钠的作用与其二硫化物(BSSB)的作用进行了比较,BSSB是硼卡醇钠在储存过程中氧化自发产生的。发现硼卡醇钠会使GFR随剂量降低,并且同样会导致UFR暂时升高。另一方面,BSSB(50mg/kg)会导致GFR大幅可逆性降低以及尿排泄减少。对一组脑肿瘤患者进行了GFR(菊粉清除率)、肾血浆流量(对氨基马尿酸清除率)和尿排泄的测量,这些患者在输注硼卡醇钠(25mg/kg体重,持续1小时)后已研究了硼的分布情况。尿量增加是主要影响(高达初始值的200%),GFR和RPF的变化意义不大,除了一名患者的GFR降低至几乎为原始值的50%。硼卡醇钠或BSSB给药后的肾功能变化可能与硼卡醇钠在肾脏中的高潴留有关。

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引用本文的文献

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Pharmacokinetics of sodium borocaptate: a critical assessment of dosing paradigms for boron neutron capture therapy.硼卡钠的药代动力学:硼中子俘获治疗给药模式的批判性评估
J Neurooncol. 2003 Mar-Apr;62(1-2):157-69. doi: 10.1007/BF02699942.