静脉注射二巯基丁二酸治疗动物路易氏剂中毒

目的：制备抗重度路易氏剂中毒静脉注射用的二巯基丁二酸类抗毒药（ＤＭＳＡ）。方法：采用两步纯化法提纯口服胶囊中ＤＭＳＡ粗品,供动物实验中静脉注射用。结果：纯度从原９３．７９％提高到９９．６８％。元素分析、红外吸收光谱、熔点测定、细菌检验及热原检查均合格。狗及大鼠路易氏剂中毒静脉注射此ＤＭＳＡ抗毒剂,效果较好。结论：口服胶囊中ＤＭＳＡ粗品经纯化后,可供静脉注射之用,抗动物路易氏剂中毒效果好,为下一步药     

口服巯基解毒剂治疗路易氏剂中毒的疗效

本文研究了二巯基丁二酸(DMSA)和二巯基丙磺酸钠(DMPS)口服给药治疗路易氏剂中毒的疗效以及口服DMSA后的吸收及排泄情况。实验证明,中毒后立即口服DMSA或DMPS 0.5mmol/kg可分别使小鼠皮下注射路易氏剂的LD_(50)从2.54mg/kg提高为15.61mg/kg和8mg/kg,接近该二药注射给药所达到的疗效。口服DMSA对抗小鼠路易氏剂LD_(100)剂量(3.5mg/kgs.c.或用,SC)中毒的ED_(50)为0.03mmol/kg,比注射给药的ED_(50)值稍高;口服DMPS对抗小鼠路易氏剂LD_(100)剂量中毒的ED_(50)为0.17mmol/kg,大约是注射给药ED_(50)值的三倍。在大鼠皮下注射路易氏剂1.5mg/kg后立即、6h、24h和48h后分别口服DMSA或DMPS 0.5mmol/kg可显著增加尿中砷的排泄,给药后第一天砷排泄量最大。通过测定大鼠口服DMSA后尿中巯基的排泄证实DMSA在胃肠道内的吸收良好,排泄速度低于静脉注射给药。     

侦检管法测定路易氏剂中毒尿中的总砷

建立了快速检测路易氏剂中毒尿中总砷的侦检管测定法。该方法的原理是:路易氏剂中毒尿中的含砷代谢物,经硼氢化钾和酒石酸作用,还原成砷化氢,砷化氢与侦检管中的三氯化金试剂反应生成紫色化合物,根据侦检管的显色长度计算出尿中总砷含量。经最佳条件选择,该法对中毒尿中总砷的最低检出限为0.02μg/ml。尿中砷含量在0.04～1.0μg/ml的范围内,与侦检管的显色长度呈线性相关,相关系数r=0.9926。该法不经消化处理样品,即可直接测定中毒尿样,具有快速、简便、灵敏和专一性较强的特点,适合于野外和基层医院应用。     

亚当氏剂全身中毒10例报告

报告了吸入高浓度亚当氏剂导致全身中毒患者１０例。吸入毒烟后除出现眼、上呼吸道刺激症状外，还有腹痛、腹泻、食欲不振、精神抑郁、全身乏力等症状，４例合并肺水肿和肺部感染，其中８例经刺激性毒剂中毒常规治疗后症状缓解，但随访１年仍有呼吸系统症状。另２例除常规治疗外，还给予口服二巯基丁二酸２ｇ／ｄ，连用７ｄ症状消失，随访无后遗症状，说明亚当氏剂中毒出现症状时，可能有砷吸收中毒，应给予驱砷治疗，驱砷诸法中以口     

芥子气－路易氏剂混合毒剂中毒特点及救治措施

糜烂性毒剂是现存化学武器的主要填充战剂,也是日本遗弃在华化学武器（简称日遗化武）的主要战剂。除常见的以单一战剂填充化学武器之外,为了能在寒区和高纬度地区使用而发展的芥子气－路易氏剂混合毒剂（简称芥路混合剂）是一种特殊而重要的战剂。该文就芥路混合剂中毒的毒理学、应急处置、临床救治等进行了介绍。     

口服二巯丁二酸驱砷治疗5例报告

二巯丁二酸(DMSA)是厂谱金属解毒剂,具有疗效高、毒性小等特点。报告了口服DMSA治疗5例急性砷中毒后期患者,在服药后第1、2d尿砷排出量有不同程度增加,5例皆治愈,且无不良反应。     

三氧化二砷治疗急性早幼粒细胞白血病

急性早幼粒细胞白血病 (APL)是一种特殊类型的急性白血病 (AL) ,属急性髓系白血病 (AML)的M3 亚型。临床上 ,其出血症状十分突出 ,发生率也很高 ,约占 72 % -94% [1] ,且常表现为弥散性血管内凝血 (DIC)而致颅内出血 ,因此早期死亡 (治疗十天以内 )率高达 11.3 % [2 ] ;若联合化疗则可达 3 0 % -4 0 % [3 ] 。1988年王振义首次报道全反式维甲酸 (ATRA)诱导分化治疗APL ,它不促发DIC ,不引起骨髓抑制 ,且可取得 85 %以上的完全缓解 (CR)率 ,[4～ 9] 明显高于联合化疗 ( 5 0 % -80 % ) ,但是维甲酸治疗伴随有维甲酸综合征[10 ] 和维…     

与二巯基丁二酸（DMSA）核素显像和最后诊断对比评价综合肾脏超声检查在儿童急性尿道感染评估肾脏损害中的价值

本研究的目的是通过与①^99TC^m，DMSA核素显像及②最后诊断进行对比，评价综合肾脏超声即结合灰阶超声和幅度编码彩色多普勒超声成像（aCDS）在评估婴幼儿尿道感染（UTI）中的价值。对287例UTI患儿进行了综合肾脏超声检查和DMSA核素显像，检查结果以①DMSA核素显像和②最后诊断为金标准，比较其诊断肾脏损害的可靠性。     

Using technetium-99m (V) dimercaptosuccinic acid to detect malignancies from single solid masses in the lungs

Fifty patients (43 male,7 female, age 31–77 years) with single solid masses in their lungs based on the findings of a chest X-radiograph [40 malignancies: 5 small cell carcinoma (Ca), 17 epidermoid Ca, 12 adeno Ca, 6 undifferentiated large cell Ca] and 10 benign lesions underwent technetium-99m (V) dimercaptosuccinic acid [^99m-(V)DMSA] scans to evaluate the usefulness of ^99mTc-(V)DMSA in the detection of lung Ca with different cell types and benign lesions. Only 43% (17/40) of the malignancies in the lungs were detected by ^99mTc-(V)DMSA, including 29% (5/17) epidermoid Ca, 50% (6/12) adeno Ca and 17% (1/6) undifferentiated large cell Ca of the lungs. However, all 5 cases of small cell Ca and 11 cases combined with bone metastasis were revealed by ^99mTc-(V)DMSA. In addition, 3 of the 10 benign lesions (2 organizing pneumonias, 1 benign tumor) presented with an uptake of ^99mTc-(V)DMSA. The diagnostic sensitivity, specificity and accuracy were 43%, 70% and 48%, respectively, in differentiating malignant from benign lesions for the single solid mass in the lungs. In conclusion, ^99mTc-(V)DMSA is of little or no use in the differentiation of lung Ca from single solid masses in the lungs. Correspondence to: C.H. Kao     

Oxygen bubbling can improve the labelling of pentavalent technetium-99m dimercaptosuccinic acid

It has previously been reported that almost all of the trivalent technetium-99m dimercaptosuccinic acid (^99mTc (III) DMSA) present in the labelling product of pentavalent technetium-99m DMSA (^99mTc (V) DMSA) can be changed into^99mTc (V) DMSA by bubbling with pure oxygen. We therefore performed studies in animals (mice) and humans to investigate the effect of such oxygen bubbling on the labelling efficiency of and on the renal uptake of^99mTc. The method of labelling of^99mTc (V) DMSA was that of Hirano. It was found that oxygen bubbling oxidized the contaminated^99mTc (III) DMSA into^99mTc (V) DMSA in vitro and decreased the uptake of radioactivity in the kidney in both animals and humans.     

Technetium-99m dimercaptosuccinic acid and ifosfamide tubular dysfunction in children with cancer

Quantitative ^99mTc-dimercaptosuccinic acid (^99mTc-DMSA) renal scintigraphy was used to asses ifosfamide-induced changes in renal function in 11 children who received chemotherapy for various malignancies. Serial measurements of absolute ^99mTc-DMSA renal uptake, calculated on conjugated views, were performed during and after chemotherapy. Data of 37 studies obtained before and at different cumulative dose levels of ifosfamide were analysed in relation to clinical and biochemical parameters. A highly significant relationship between ^99mTc-DMSA uptake and cumulative ifosfamide dose was found (P<0.001). The most frequently observed abnormal pattern on scintigraphic images was decreased kidney uptake together with increased accumulation in bladder. ^99mTc-DMSA uptake was more consistent than ₂-microglobulin values in urine and more sensitive than quantitative hyperaminoaciduria and tubular resorption of phosphate for the detection of ifosfamide-induced tubular dysfunction. ^99mTc-DMSA uptake was decreased in both patients with and patients without clinical toxicity. Persistently reduced ^99mTc-DMSA uptake was observed in four patients during follow-up; in one of them, who was asymptomatic after ifosfamide therapy, sudden onset of Fanconi syndrome was observed when he was retreated with carboplatin 1 year later. It is concluded that ^99mTc-DMSA renal scintigraphy is a suitable method to assess progressive ifosfamide-induced tubular injury whereas scintigraphic imaging is helpful for interpreting renal uptake changes. The test is able to detect subclinical injury and may potentially predict high risk at retreatment.     

In vitro and in vivo studies with pentavalent technetium-99m dimercaptosuccinic acid

The purpose of this investigation was to characterise the in vivo chemistry and binding mechanisms of technetium-99m dimercaptosuccinic acid [^99mTc(V)DMSA]. Biodistribution was studied in mice by frozen section whole-body autoradiography and microautoradiography in selected tissues. Binding to bone mineral analogues was studied in vitro using various forms of calcium phosphate and hydroxyapatite under varied conditions. Similar studies with^99mTc-hydroxymethylene diphosphonate (HDP) were also carried out for comparison. The in vivo stability of^99mTc(V)DMSA was monitored by high-performance liquid chromatographic analysis of blood and urine samples taken over 24 h from patients injected with the tracer. Whole-body autoradiography shows that^99mTc(V)DMSA has highest affinity for bone (cortical rather than medullary) in mice. Substantial uptake of the tracer was also observed in the kidney (cytoplasm of cortical renal tubular cells). No specific localisation was observed in the liver at either the microscopic or the macroscopic level. While^99mTc-HDP bound strongly to calcium phosphates under all conditions,^99mTc(V)DMSA binding was inhibited in the presence of phosphate and was stronger at pH 6.0 than at pH 7.4. In non-phosphate buffers, however, the binding of^99mTc(V)DMSA remained high across the pH range 4–7.4.^99mTc(V)DTVISA binds to calcium phosphates chemically unaltered, and no radioactive species other than the three isomers of^99mTc(V)DMSA were detected in blood or urine samples taken from patients up to 24 h after injection.^99mTc(V)DMSA is stable in vivo, and no conversion of the complex to other chemical species needs to be invoked to explain its uptake in bone metastases or soft tissue tumour. Bone affinity may be due to reversible binding of the unaltered complex to the mineral phase of bone.     

Normal appearances of technetium-99m dimercaptosuccinic acid in children on planar imaging

Thirty-two children who underwent renal arteriography with normal results also underwent technetium-99m dimercaptosuccinic acid (DMSA) imaging. Variations in the normal appearance of ^99mTc-DMSA images are described in these children. Criteria for high-quality ^99mTc DMSA images are defined in terms of kidney outline and contrast between the inner and the outer part of the kidney. Most of the images in this study were of high quality. The two most common features of normal ^99mTc-DMSA images were a round-shaped (50%) or flat (either lateral or medial aspect) (24.8%) contour. A small number of unusual appearances were observed and these have been illustrated. The mean differential function of the left kidney was 51% with a range of 45%–57%. Received 9 October 1998 and in revised form 5 January 1999     

Technetium-99m diethylene triamine penta-acetic acid and dimercaptosuccinic acid in the detection of a segmental branch stenosis of the renal artery by captopril renography

We present a case in which a 39-year-old woman with correctable bilateral renovascular hypertension did not show abnormality during post-captopril technetium-99m dimercaptosuccinic acid (DMSA) study. Post-captopril ^99mTc-diethylene triamine pentaacetic acid (DTPA) scintigraphy revealed the adverse effect of a stenosis of the artery supplying the upper part of her left kidney but failed to uncover the existence of severe multiple narrowings of the right renal artery. After bilateral renovascular reconstructive surgery, the hypertension completely disappeared. This case illustrates that DTPA may be more efficacious than DMSA in the detection of segmental loss of renal function induced by angiotensin converting enzyme inhibition. Offprint requests to: L. Bajnok     

Preparation and clinical evaluation of technetium-99m dimercaptosuccinic acid for tumour scintigraphy

We describe a simple method of pentavalent technetium-99m dimercaptosuccinic acid [^99mTc(V)-DMSA] preparation for the imaging of medullary carcinoma of the thyroid using commercially available kits. ^99mTc(V)-DMSA is available at high pH (approximately 7.5) by adding NaHCO₃ solution in the presence of a small amout of reducing agent (SnCl₂). On the other hand, trivalent ^99mTc-DMSA [^99m-Tc(III)-DMSA] can be obtained at low pH (below 3) in the presence of an excess amount of reducing agent. In the clinical evaluation of a patient with a medullary carcinoma of the thyroid, only ^99mTc(V)-DMSA revealed an area of intense accumulation.     

Development of a radiopharmaceutical activity schedule for technetium-99m dimercaptosuccinic acid in children based on image quality criteria

The aim of this study was to determine an activity schedule (amount of administered activity in relation to body weight) for technetium-99m dimercaptosuccinic acid examinations in children, from information present in renal scintigraphic images. Scans from 48 children (5 weeks to 14.8 years old) were graded for image quality according to the clarity of both kidney outline and internal structure. Numerical image data (kidney and background counts, signal-to-noise ratio) were associated with these subjective gradings to formulate three criteria, specifying the required values of the above-measured parameters to yield optimum grades of image quality. When applied to derived functions, a kidney uptake of 20% was required to satisfy the criterion based on the signal-to-noise ratio. Using this value with the other two criteria predicts the form of the weight-dependent activity schedule as a function of imaging time. Examples of schedules for imaging times of 300 and 600 s are compared with a schedule based on surface area. Received 21 March and in revised form 5 July 1997