Department of Pharmaceutical Sciences, Linus Pauling Institute, Oregon State University, Corvallis, Oregon 97331, USA.
Department of Anesthesiology, University of Illinois, Chicago, Illinois 60612, USA.
Toxicol Sci. 2024 Jun 26;200(1):137-145. doi: 10.1093/toxsci/kfae053.
Administration of high-dose vitamin K1 (VK1) overcomes coagulopathy and bleeding elicited by acute poisoning with long-acting anticoagulant rodenticides (LAARs). However, long-term (months) treatment is required due to long LAAR biological half-lives that may lead to poor compliance and recurrent coagulopathy. The half-lives of LAARs are extended by slow metabolism, and similar to warfarin, are thought to undergo enterohepatic recirculation. We now show that treatment with the bile acid sequestrant cholestyramine (CSA) administered concomitantly with VK1 decreases plasma LAAR levels and increases LAAR fecal excretion. Daily CSA treatment for 14 days did not reduce plasma VK1 levels, or increase prothrombin time. Collectively, these data show that CSA accelerates LAAR clearance from rabbits without adverse effects on VK1 anticoagulation, and could provide an additional therapeutic option for treatment of LAAR poisoning.
大剂量维生素 K1(VK1)的给药可克服长效抗凝血灭鼠剂(LAARs)急性中毒引起的凝血功能障碍和出血。然而,由于 LAAR 的生物半衰期较长(数月),可能导致依从性差和反复发生凝血功能障碍,因此需要长期(数月)治疗。LAAR 的半衰期通过缓慢的代谢而延长,并且与华法林类似,被认为会经历肠肝再循环。我们现在表明,同时给予胆汁酸螯合剂考来烯胺(CSA)与 VK1 治疗可降低血浆 LAAR 水平并增加 LAAR 的粪便排泄。连续 14 天的 CSA 治疗并未降低血浆 VK1 水平,也未延长凝血酶原时间。总的来说,这些数据表明 CSA 可加速从兔子中清除 LAAR,而不会对 VK1 抗凝产生不利影响,并且可能为 LAAR 中毒的治疗提供另一种治疗选择。