Osterloh J, Becker C E
Clin Pharmacol Ther. 1986 Dec;40(6):686-93. doi: 10.1038/clpt.1986.245.
The pharmacokinetics of 1 gm intramuscular doses of CaNa2 (14C-)EDTA and the chelation of lead (Pb) were studied in 10 subjects with varying degrees of renal function and normal body burdens of Pb. The clearance of CaNa2EDTA significantly correlated with creatinine clearances (CLCR) (r = 0.8373; P = 0.0097). Clearances were decreased in subjects with CLCR less than 70 ml/min as compared with subjects with CLCR greater than 100 ml/min (28 vs. 76 ml/min). Maximum serum CaNa2EDTA concentrations and volume of distribution (Varea) (0.05 to 0.23 L/kg) were similar in all subjects. The Varea is smaller than previously described and is more consistent with other experimental data. Considering all subjects, initial blood Pb concentrations correlated with cumulative urine Pb excretion over 3 days (r = 0.8967; P = 0.0005). Urine Pb excretion did not correlate with measures of renal function or measures of CaNa2EDTA kinetics. Subjects with abnormal CLCR showed significantly greater decreases in blood Pb from day 1 to day 4 (7.0 micrograms/dl vs. 1.2 micrograms/dl) compared with normal subjects. These decreases in blood Pb correlated with CLCR (r = 0.7774; P = 0.138) and urine protein (r = 0.8435; P = 0.0087) but not with urine Pb excretion. Renal dysfunction may alter Pb chelatability, bone-blood Pb reequilibration, PbEDTA distribution, or PbEDTA excretion.
对10名肾功能程度各异且体内铅（Pb）负荷正常的受试者，研究了1克肌肉注射剂量的CaNa2 (14C-)EDTA的药代动力学以及铅（Pb）的螯合情况。CaNa2EDTA的清除率与肌酐清除率（CLCR）显著相关（r = 0.8373；P = 0.0097）。与CLCR大于100 ml/分钟的受试者相比，CLCR小于70 ml/分钟的受试者清除率降低（28对76 ml/分钟）。所有受试者的血清CaNa2EDTA最高浓度和分布容积（Varea）（0.05至0.23 L/kg）相似。Varea比先前描述的小，且与其他实验数据更一致。综合所有受试者，初始血铅浓度与3天内累积尿铅排泄相关（r = 0.8967；P = 0.0005）。尿铅排泄与肾功能指标或CaNa2EDTA动力学指标无关。与正常受试者相比，CLCR异常的受试者从第1天到第4天血铅下降幅度显著更大（7.0微克/分升对1.2微克/分升）。这些血铅下降与CLCR（r = 0.7774；P = 0.138）和尿蛋白（r = 0.8435；P = 0.0087）相关，但与尿铅排泄无关。肾功能障碍可能会改变铅的螯合能力、骨 - 血铅再平衡、PbEDTA分布或PbEDTA排泄。
