Frequency of adverse reactions to radiopharmaceuticals in Europe

A prospective survey was performed in 17 nuclear medicine departments during 1996 in an attempt to provide reliable data on the prevalence of adverse reactions to radiopharmaceuticals. All adverse events following radiopharmaceutical administration were recorded, irrespective of the severity or likelihood of causality, and subsequently analysed using an algorithm developed by Silberstein et al., designed to establish a cause-effect relationship. A prevalence of 11 events per 105 administrations was obtained (95% confidence limits 3.3–19.2). No serious of life-threatening events were reported. This rate is slightly higher than that obtained in a larger scale study in the United States (2.3 events per 105 administrations, 95% confidence limits 1.2–3.4). The difference may be due to the decision to include or exclude vasovagal events from the analysis, the way in which the algorithm was used and the comparative size and time scale of the two studies. The prevalence of adverse reactions is approximately 1000-fold than less that occurring with iodinated contrast media and drugs.     

Copper radionuclides and radiopharmaceuticals in nuclear medicine

The chemistry, radiochemistry, radiobiology, and radiopharmacology of radiopharmaceuticals containing copper radionuclides are reviewed. Copper radionuclides offer application in positron emission tomography, targeted radiotherapy, and single photon imaging. The chemistry of copper is relatively simple and well-suited to radiopharmaceutical application. Current radiopharmaceuticals include biomolecules labelled via bifunctional chelators primarily based on cyclic polyaminocarboxylates and polyamines, and pyruvaldehyde-bis(N⁴-methylthiosemicarbazone) (PTSM) and its analogues. The chemistry of copper, of which only a fraction has yet been exploited, is likely to be applied more fully in the future.     

Myocardial scintigraphy — 25 years after start

The development of myocardial scintigraphy (MS) reflects the clinical success of a representative procedure in nuclear medicine. Radiopharmaceuticals for visualizing vital and damaged myocardium and techniques (planar-qualitative, planar-quantitative, SPECT-qualitative — quantitative with comparative sensitivities) are briefly reviewed with the main focus on their clinical application in coronary (CHD) and noncoronary heart disease, where recent literature from the United States and Europe is considered. The limited value of MS for screening of CHD is outlined and its present and future role in detecting asymptomatic (silent) ischemia/infarction and asymptomatic patients at professional risk is stressed. The present state of MS in coronary heart disease is discussed for single and multivessel disease, previous infarction, and risk stratification (myocardial washout, pulmonary uptake, ischemic dilation, absent heart sign), reflecting the importance of the procedure in exercise-induced ischemia as well as in ischemia at rest for prognostication of the natural and therapeutic course, i.e., therapy control (angioplasty, bypass, lysis, cardiac drugs). More marginal but upcoming clinical indications are mentioned, such as progressive systemic sclerosis, cardiac transplantation, pediatric cardiology, and problems of nephrology/urology. The normal values and the impact of digital radiology and of contrast cardiography are touched upon. Preliminary cases with ¹¹¹In-antimyosin and ^99mTc-Isonitriles are presented including correlative results between global ejection fraction determination according to gated ^99mTc-isonitrile and conventional ^99mTc-erythrocyte ventriculogram (r=0,75; n=10).Dedicated to Prof. Heinz Hundeshagen on the occasion of his 60th birthday     

α粒子放射性药物在骨转移瘤治疗中的应用进展

骨骼是晚期恶性肿瘤的常见转移部位之一,骨转移瘤不仅会导致顽固性骨痛、病理性骨折等骨相关事件（SRE）的发生,还会导致医疗费用的增加和死亡风险的上升。放射性药物内放射治疗具有疗效好、靶向性好和毒性低等优点。常用于治疗骨转移瘤的放射性药物主要是释放β粒子和α粒子的药物,其中释放β粒子的放射性药物的临床应用较成熟,但也具有一定的局限性。近年来,释放α粒子的放射性药物越来越多地用于骨转移瘤的治疗,其在缓解骨痛、降低SRE发生率、延长总生存期等方面具有更大的优势。笔者仅就α粒子放射性药物在骨转移瘤治疗中的应用进展进行综述。     

全身骨显像剂注射方法对剂量准确性和辐射防护的影响

目的研究单光子发射型计算机断层成像术(SPECT)全身骨显像患者采用不同注射方法注射显像剂对放射性药物剂量准确性和辐射防护的影响。方法 按随机数字表,将行SPECT全身骨显像的100例患者分为两组,每组50例。其中研究组采用抽回血注射法,对照组采用头皮针注射法,显像前2～3h两组均注射99mTC-亚甲基二磷酸盐(MDP)作为显像剂,剂量20mci(740MBq),体积0.5ml。A、B两组注射后均立即用Χ-Υ辐射仪测量注射器及针头内残留放射性药物的残余辐射量,用活度计测量残留放射性药物的残余放射性活度,并记录静脉注药时间。结果研究组注射后注射器内的残余放射性活度及残余辐射量均低于对照组,差异有统计学意义(P<0.01);研究组注药时间短于对照组,差异也有统计学意义(P<0.01)。结论抽回血注射法与头皮针注射法相比,既减少了注射器内放射性药物的残留量和残余放射性活度,保证了成像质量,也缩短了注射人员接触射线的剂量和时间,有利于辐射防护。     

PET and PET/CT in endocrine tumours

Functional information provided by PET tracers together with the superior image quality and the better data quantification by PET technology had a changing effect on the significance of nuclear medicine in medical issues. Recently introduced hybrid PET/CT systems together with the introduction of novel PET radiopharmaceuticals have contributed to the fact that nuclear medicine has become a growing diagnostic impact on endocrinology. In this review imaging strategies, different radiopharmaceuticals including the basic mechanism of their cell uptake, and the diagnostic value of PET and PET/CT in endocrine tumours except differentiated thyroid carcinomas will be discussed.     

放射性药物自动分装仪装置设计

随着我国医疗事业尤其是核医学事业的迅猛发展,大量的核医学设备在被广泛地应用到医疗实践的过程中,该类设备检查用核素的种类及数量越来越多。相关放射工作人员在使用核素时需要对其进行分装,基本采用手工分装方式。这种长时间在辐射环境下的工作必然给相关医疗工作人员的健康带来危害。如何预防辐射成为关注的焦点。本文基于此,设计了一种放射性药物自动分装仪,它由PLC控制整个系统,由步进电机、触摸屏伺服电机、气动元件附以一定的机械装置构成,能够对临床所需的核素剂量进行精确的分装,降低了工作人员接受辐射的强度,有效地解决了辐射问题。     

Comparisons of labeling efficiency,biological activity and biodistribution among 125I-, 67Ga-DTPA-and 67Ga-DFO-lectins

The labeling efficiency, biological activity and biodistribution of ¹²⁵I labeled and ⁶⁷Ga chelating agent conjugated lectins were investigated. Pisum sativum agglutinin (PSA) and Lens culinaris agglutinin (LCH) were efficiently labeled with ⁶⁷Ga using bifunctional chelating agents such as diethylenetriaminepentaacetic acid (DTPA) and deferoxamine (DFO), whereas labeling with ¹²⁵I was significantly less efficient. The agglutinating activity of these lectins towards Ehrlich ascites tumor (EAT) cells was retained on conjugation with DFO, but not with DTPA. The in vitro binding ratio of ⁶⁷Ga-DFO-lectins for EAT cells was almost the same as that of ¹²⁵I-lectins. However, the value was significantly decreased in the case of ⁶⁷Ga-DTPA-lectins. In the biodistribution study of radiolabeled lectins in Ehrlich solid tumor (EST) bearing mice, the accumulation of radioactivity in tumor tissue was very much less with ⁶⁷Ga-DTPA-lectins than with ¹²⁵I-lectins. However, the concentration was significantly elevated in the case of ⁶⁷Ga-DFO-lectins. While, these lectins accumulated in liver, spleen, lung, and kidney to a greater extent than ⁶⁷Ga citrate, the tumor to organ ratios became very low. These low tumor to organ ratios, in contrast to ⁶⁷Ga citrate, will certainly inhibit the tumor delineation, and therefore it seems that in spite of a high accumulation ratio of ⁶⁷Ga-DFO-lectins in tumor tissue, these agents are not useful in tumor detection.     

Rhenium-188 and technetium-99m nitridobis(N-ethoxy-N-ethyldithiocarbamate) leucocyte labelling radiopharmaceuticals: [ReN(NOET)2] and [TcN(NOET)2], NOET = Et(EtO)NCS2: Their in vitro localization and chemical behaviour

In this study, we have investigated the preparation of rhenium-188 nitridobis(N-ethoxy-N-ethyldithiocarbamate) [¹⁸⁸ReN(NOET)₂] (NOET = Et(EtO)NCS₂), analogous to the known technetium-99m radiopharmaceutical. The new ¹⁸⁸Re complex was synthesized in good yield with a satisfactory radiochemical purity, using a kit method. The subcellular localization of both radiopharmaceuticals in granulocytes was observed by microautoradiography. The uptake was independent of the radionuclide and predominantly nuclear. Furthermore, HPLC was used to characterize the ^99mTc complex before and after blood cell labelling and revealed that the intact radiopharmaceutical was involved.     

用于PET放射性药物合成的微流体芯片

微流体芯片在有机合成领域显示了它独特的优势,而应用到放射性药物合成领域却很少.最近,国际上几个科研小组证实了微流体芯片在放射性药物合成上的潜力,并证实传统放射合成的许多步骤均可被微流体芯片所取代.同时也证实以微流体芯片为基础的放射性化学合成比传统的放射性化学合成使用的前体量更少,反应速度更快,合成出的药品有更高的比活度和产率,纯化过程也更简单,同时对放射性的防护也更容易.尽管有如此多的优点,但目前还没有被广泛的商业开发.本文对目前国际上主要的几种微流体芯片的优缺点及其在PET药物合成中的应用进行了综述.