Gadolinium-containing MRI contrast agents: important variations on a theme for NSF.
Gadolinium-containing MRI contrast agents: important variations on a theme for NSF.
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DOI：
10.1016/j.jacr.2007.08.014
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发表时间：
2008-01-01
期刊：
影响因子：
--
通讯作者：
Kuo, Phillip H
中科院分区：
文献类型：
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作者：
Kuo, Phillip H
为了提高磁共振成像的临床应用，每年要使用数百万剂量的钆基造影剂（gbca）。所有被批准的药物都将稀土金属钆的一个原子加入到螯合物中，以提高通常有毒的游离钆的安全性。尽管gpca具有临床互换性，但gpca与肾源性系统性纤维化（NSF）之间不可否认的流行病学联系促使人们重新研究gpca的不同化学性质。基于钆的造影剂可以分为不同的类别：线性与大环结构，离子与非离子，非蛋白质结合剂与蛋白质结合剂。GBCAs在金属转化、动力学和热力学稳定性方面存在显著差异，因此它们倾向于释放游离钆，这被认为是诱发NSF的原因。gadodiamide易发生金属转化，且热力学和动力学稳定性相对较低，与大多数NSF病例有关，这支持了这一假设。另一方面，更大的稳定性的大环剂假设将赋予更大的安全边际有关NSF。由于很少有关于NSF实验模型的公开数据存在，因此有必要继续保持警惕，以报告新的NSF病例，特别是关于小市场份额的代理商。
Millions of doses of gadolinium-based contrast agents (GBCAs) are administered annually to improve the clinical utility of magnetic resonance imaging. All the approved agents incorporate one atom of the rare earth metal gadolinium into a chelate to improve the safety of the ordinarily toxic free gadolinium. The undeniable epidemiologic link between GBCAs and nephrogenic systemic fibrosis (NSF) has prompted renewed investigation into the different chemical properties of the GBCAs despite their clinical interchangeability. Gadolinium-based contrast agents can be divided into different categories: linear versus macrocyclic structure, ionic versus nonionic, and non-protein-binding versus protein-binding agents. The GBCAs differ significantly with respect to transmetallation and kinetic and thermodynamic stability and therefore their propensity to release free gadolinium, which is hypothesized to induce NSF. That gadodiamide, with its susceptibility to transmetallation and relatively low thermodynamic and kinetic stability, is associated with the most cases of NSF supports this hypothesis. On the other hand, the greater stability of a macrocyclic agent hypothetically would confer a greater safety margin with regard to NSF. Because few published data on an experimental model of NSF exist, continuing vigilance is necessary to report new cases of NSF, especially with regard to the agents with small market share.