Kapoor S C, Wielopolski L, Graziano J H, LoIacono N J
Department of Pharmacology, Columbia University, College of Physicians and Surgeons, New York, New York 10032.
Toxicol Appl Pharmacol. 1989 Mar 1;97(3):525-9. doi: 10.1016/0041-008x(89)90257-3.
2,3-Dimercaptosuccinic acid (DMSA) is a new orally active heavy metal chelator for the treatment of childhood Pb intoxication on an outpatient basis. The influence of DMSA, as well as other chelating agents, on gastrointestinal 203Pb absorption and whole-body 203Pb retention was examined. Groups of Sprague-Dawley rats (230-260 g) were gavaged with a solution containing approximately 25 mg/kg Pb [as Pb(NO3)2] plus 15 microCi 203Pb. Some groups were then immediately given 0.11 mmol/kg of either DMSA, CaNa2EDTA, D-penicillamine, or BAL by oral gavage, while other groups received the same drugs by ip injection. Control groups received solutions of the drug vehicles po or ip. Whole-body Pb retention and gastrointestinal Pb absorption (whole body retention + urinary Pb excretion) were significantly decreased in rats that received DMSA po. This finding implies that the use of DMSA to treat childhood lead intoxication on an outpatient basis is not associated with a risk for increased Pb absorption.
2,3-二巯基丁二酸(DMSA)是一种新型口服活性重金属螯合剂,用于门诊治疗儿童铅中毒。研究了DMSA以及其他螯合剂对胃肠道203Pb吸收和全身203Pb潴留的影响。将Sprague-Dawley大鼠(230-260克)分组,用含有约25毫克/千克铅[以Pb(NO3)2形式]加15微居里203Pb的溶液灌胃。然后,一些组立即通过口服灌胃给予0.11毫摩尔/千克的DMSA、CaNa2EDTA、D-青霉胺或二巯丙醇,而其他组通过腹腔注射给予相同药物。对照组经口或腹腔注射给予药物赋形剂溶液。口服DMSA的大鼠全身铅潴留和胃肠道铅吸收(全身潴留+尿铅排泄)显著降低。这一发现表明,门诊使用DMSA治疗儿童铅中毒与铅吸收增加的风险无关。