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急性或长期放射性碘暴露情况下稳定碘或高氯酸盐对甲状腺的保护作用比较。

A comparison of thyroidal protection by stable iodine or perchlorate in the case of acute or prolonged radioiodine exposure.

机构信息

Bundeswehr Institute of Radiobiology, Neuherberg Str. 11, 80937, Munich, Germany.

Japan Self Defense Forces National Defense Medical College Research Institute, Tokorozawa, Japan.

出版信息

Arch Toxicol. 2020 Sep;94(9):3231-3247. doi: 10.1007/s00204-020-02809-z. Epub 2020 Jul 12.

Abstract

In the case of a nuclear power plant accident, repetitive/prolonged radioiodine release may occur. Radioiodine accumulates in the thyroid and by irradiation enhances the risk of cancer. Large doses of non-radioactive iodine may protect the thyroid by inhibiting radioiodine uptake into the gland (iodine blockade). Protection is based on a competition at the active carrier site in the cellular membrane and the Wolff-Chaikoff effect, the latter being, however, only transient (24-48 h). Perchlorate may alternatively provide protection by a carrier competition mechanism only. Perchlorate has, however, a stronger affinity to the carrier than iodide. Based on an established biokinetic-dosimetric model developed to study iodine blockade, and after its extension to describe perchlorate pharmacokinetics and the inhibition of iodine transport through the carrier, we computed the protective efficacies that can be achieved by stable iodine or perchlorate in the case of an acute or prolonged radioiodine exposure. In the case of acute radioiodine exposure, perchlorate is less potent than stable iodine considering its ED A dose of 100 mg stable iodine has roughly the same protective efficacy as 1000 mg perchlorate. For prolonged exposures, single doses of protective agents, whether stable iodine or perchlorate, offer substantially lower protection than after acute radioiodine exposure, and thus repetitive administrations seem necessary. In case of prolonged exposure, the higher affinity of perchlorate for the carrier in combination with the fading Wolff-Chaikoff effect of iodine confers perchlorate a higher protective efficacy compared to stable iodine. Taking into account the frequency and seriousness of adverse effects, iodine and perchlorate at equieffective dosages seem to be alternatives in case of short-term acute radioiodine exposure, whereas preference should be given to perchlorate in view of its higher protective efficacy in the case of longer lasting radioiodine exposures.

摘要

在核电站事故的情况下,可能会发生重复/长时间的放射性碘释放。放射性碘会在甲状腺中积聚,并通过辐射增加癌症的风险。大剂量的非放射性碘可以通过抑制碘进入腺体(碘阻断)来保护甲状腺。这种保护基于细胞膜上的主动载体部位的竞争和 Wolff-Chaikoff 效应,后者只是暂时的(24-48 小时)。高氯酸盐也可以通过载体竞争机制提供保护。然而,高氯酸盐与载体的亲和力比碘强。基于为研究碘阻断而建立的生物动力学剂量模型,并对其进行扩展以描述高氯酸盐药代动力学和抑制碘通过载体的运输,我们计算了在急性或长时间放射性碘暴露的情况下,稳定碘或高氯酸盐可以实现的保护效率。在急性放射性碘暴露的情况下,考虑到稳定碘的 ED 剂量为 100mg,高氯酸盐的效力比稳定碘低,1000mg 高氯酸盐的保护效果大致与 100mg 稳定碘相同。对于长时间暴露,保护剂的单次剂量,无论是稳定碘还是高氯酸盐,提供的保护都远低于急性放射性碘暴露后的保护,因此需要重复给药。在长时间暴露的情况下,高氯酸盐与载体的亲和力较高,加上碘的 Wolff-Chaikoff 效应逐渐消失,使得高氯酸盐的保护效率比稳定碘高。考虑到不良反应的频率和严重程度,在短期急性放射性碘暴露的情况下,碘和高氯酸盐在等效剂量下似乎是替代品,而鉴于高氯酸盐在长时间放射性碘暴露的情况下具有更高的保护效率,应优先考虑高氯酸盐。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cbc5/7415763/226f2295bf5e/204_2020_2809_Fig1_HTML.jpg

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