Int J Clin Pharmacol Ther. 2021 Feb;59(2):89-98. doi: 10.5414/CP203858.
To explore the mode of action (MoA) by which sugammadex interferes with coagulation.
The effect of sugammadex on various steps in the coagulation cascade including thrombin generation, factor Xa activity, and factor Xa generation was explored in human plasma.
Sugammadex did not affect a conventional thrombin generation test (TGT), while it prolongs activated partial thromboplastin time (APTT) and prothrombin time (PT). However, a customized TGT with PT reagent revealed sugammadex effects. In addition, sugammadex prolonged a one-step prothrombinase-induced clotting time (PiCT) using human factor Xa. Furthermore, sugammadex interfered with factor Xa generation induced by an intrinsic and not by an extrinsic activator, nor by Russell's viper venom factor X (RVV-X).
Adapted, rather than standard, experiments show that sugammadex is likely to decrease factor Xa activity in the common pathway and activation of factor X specifically in the intrinsic pathway.
探讨琥珀酸舒更葡糖钠干扰凝血的作用机制（MoA）。
在人血浆中，研究了琥珀酸舒更葡糖钠对凝血级联反应的各个步骤（包括凝血酶生成、因子 Xa 活性和因子 Xa 生成）的影响。
琥珀酸舒更葡糖钠不影响常规凝血酶生成试验（TGT），但延长活化部分凝血活酶时间（APTT）和凝血酶原时间（PT）。然而，使用凝血酶原试剂的定制 TGT 显示出琥珀酸舒更葡糖钠的作用。此外，琥珀酸舒更葡糖钠延长了一步法凝血酶原酶诱导的凝血时间（PiCT）。此外，琥珀酸舒更葡糖钠干扰了由内在激活剂而非外在激活剂、或由 Russell's viper venom factor X（RVV-X）诱导的因子 Xa 生成。
适应性而非标准实验表明，琥珀酸舒更葡糖钠可能会降低共同途径中的因子 Xa 活性，并特异性地激活内在途径中的因子 X。
