市售5-氟尿嘧啶药瓶的心脏毒性源于该药物的碱水解。
Cardiotoxicity of commercial 5-fluorouracil vials stems from the alkaline hydrolysis of this drug.
作者信息
Lemaire L, Malet-Martino M C, de Forni M, Martino R, Lasserre B
机构信息
Laboratoire des IMRCP, Université Paul Sabatier, Toulouse, France.
出版信息
Br J Cancer. 1992 Jul;66(1):119-27. doi: 10.1038/bjc.1992.227.
Abstract
The cardiotoxicity of 5-fluorouracil (FU) was attributed to impurities present in the injected vials. One of these impurities was identified as fluoroacetaldehyde which is metabolised by isolated perfused rabbit hearts into fluoroacetate (FAC), a highly cardiotoxic compound. FAC was also detected in the urine of patients treated with FU. These impurities were found to be degradation products of FU that are formed in the basic medium employed to dissolve this compound. To avoid chemical degradation of this antineoplastic drug, the solution of FU that will be injected should be prepared immediately before use.
摘要
5-氟尿嘧啶（FU）的心脏毒性归因于注射瓶中存在的杂质。其中一种杂质被鉴定为氟乙醛，它在离体灌注的兔心脏中代谢为氟乙酸（FAC），这是一种具有高度心脏毒性的化合物。在用FU治疗的患者尿液中也检测到了FAC。这些杂质被发现是FU在用于溶解该化合物的碱性介质中形成的降解产物。为避免这种抗肿瘤药物的化学降解，即将注射的FU溶液应在使用前立即配制。
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