Karras Spiros, Memi Eleni, Kintiraki Evangelia, Krassas Gerasimos E
Department of Endocrinology, Diabetes and Metabolism, Panagia General Hospital, Thessaloniki, Greece.
J Pediatr Endocrinol Metab. 2012;25(7-8):623-30. doi: 10.1515/jpem-2012-0059.
Propylthiouracil (PTU), carbimazole (CMZ) and methimazole (MMI) are the most common drugs used today in cases of adolescent thyrotoxicosis. Skepticism has been growing regarding the use of PTU in childhood and its association with severe liver failure. The aim of this review is to present all the recent data regarding pathogenesis of PTU hepatotoxicity in children and adolescents. Specifically, reactive drug metabolites and increased oxidative stress can directly activate inflammatory and immunological pathways. Drugs are not only immunogenic because of their chemical reactivity but also because they may bind through electrostatic forces to available T-cell receptors. Redox modulation is also a key regulatory strategy in the adaptive immune system. Subtle changes in the extracellular redox status may cause profound functional changes in redox-sensitive proteins. Genetic factors that affect drug biotransformation could also be implicated in this mechanistic model of PTU-related hepatotoxicity. Further studies are needed to fully understand the pathophysiology of PTU-induced liver damage.
丙硫氧嘧啶(PTU)、卡比马唑(CMZ)和甲巯咪唑(MMI)是目前青少年甲状腺毒症病例中最常用的药物。对于PTU在儿童中的使用及其与严重肝衰竭的关联,人们的怀疑日益增加。本综述的目的是呈现关于儿童和青少年PTU肝毒性发病机制的所有最新数据。具体而言,反应性药物代谢产物和氧化应激增加可直接激活炎症和免疫途径。药物不仅因其化学反应性具有免疫原性,还因其可能通过静电力与可用的T细胞受体结合。氧化还原调节也是适应性免疫系统中的关键调节策略。细胞外氧化还原状态的细微变化可能导致氧化还原敏感蛋白发生深刻的功能变化。影响药物生物转化的遗传因素也可能与PTU相关肝毒性的这一机制模型有关。需要进一步研究以充分了解PTU诱导肝损伤的病理生理学。