Paraquat (PQ) is a toxic, organic herbicide for which there is no specific antidote. Although banned in some countries, it is still used as an irreplaceable weed killer in others. The lack of understanding of the precise mechanism of its toxicity has hindered the development of treatments for PQ exposure. While toxicity is thought to be related to PQ-induced oxidative stress, antioxidants are limited in their ability to ameliorate the untoward biological responses to this agent. Summarized in this review are data on the absorption, distribution, metabolism, excretion, and toxicity (ADME/T) of PQ, focusing on the essential roles of individual transporters and enzymes in these processes. Based on these findings, strategies are proposed to design and test specific and effective antidotes for the clinical management of PQ poisoning.

百草枯 (PQ) 是一种有毒的有机除草剂，没有特效解毒剂。虽然在一些国家被禁止，但在其他国家仍然被用作不可替代的除草剂。对其毒性的确切机制缺乏了解阻碍了 PQ 暴露治疗的发展。虽然毒性被认为与 PQ 诱导的氧化应激有关，但抗氧化剂在改善对该药物不利的生物反应方面的能力有限。本综述总结了 PQ 的吸收、分布、代谢、排泄和毒性 (ADME/T) 的数据，重点关注个体转运蛋白和酶在这些过程中的重要作用。基于这些发现，提出策略来设计和测试用于 PQ 中毒临床管理的特异性和有效解毒剂。