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模拟奥沙利铂生物转化处理奥沙利铂外渗的管理。

Management of extravasation of oxaliplatin by mimicking its biotransformation.

机构信息

Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Bezmialem Vakif University, Fatih, 34093, Istanbul, Turkey.

Department of Medical Oncology, Medicana International Istanbul Hospital, Istanbul, Turkey.

出版信息

Clin Transl Oncol. 2018 Oct;20(10):1353-1357. doi: 10.1007/s12094-018-1854-z. Epub 2018 Apr 27.

Abstract

Although oxaliplatin (Oxali) plays a key role in the treatment of many types of cancer and has been reported to be an irritant, there is no specific and effective method for its extravasation and failure in Oxali extravasation management results in the need for plastic surgery. In the body, Oxali bio-transforms upon dilution in chloride-containing buffer salts to its di-chloro derivative and loses an oxalate molecule. Consequently, the chloride ions exchange with water molecules in the intracellular environment to produce the di-aqua derivative, which is the most active biotransformation product of Oxali in terms of forming the DNA adducts. Thus, inhibiting transformation of di-chloro to di-aqua derivatives by accumulating chloride ions at the site of extravasation and saturating the Oxali molecule with these ions is a strategy that could help manage extravasation. Injecting normal saline at this site is a simple yet effective way to achieve this goal.

摘要

奥沙利铂(Oxali)在治疗多种癌症中发挥着关键作用,虽然已被报道为刺激性药物,但对于其外渗目前尚无特定且有效的处理方法,而奥沙利铂外渗处理失败则可能需要进行整形手术。在体内,奥沙利铂在含氯离子缓冲盐中的稀释过程中会发生双氯代物生物转化,并失去一个草酸盐分子。因此,氯离子会在细胞内环境中与水分子交换,产生双水合衍生物,这是奥沙利铂在形成 DNA 加合物方面最具活性的生物转化产物。因此,通过在渗漏部位积累氯离子并使这些离子饱和奥沙利铂分子,从而抑制双氯代物向双水合衍生物的转化,是一种有助于处理外渗的策略。在该部位注射生理盐水是实现这一目标的简单而有效的方法。

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