Schulman Sam
Coagulation Unit, Department of Medicine, Karolinska Hospital, Stockholm, Sweden.
Semin Thromb Hemost. 2003 Dec;29 Suppl 1:33-6. doi: 10.1055/s-2003-45415.
The rapid development of new and selective anticoagulant agents has triggered the question of which activated coagulation factor would be a better target for the inhibition of coagulation. Indirect comparisons between studies on the different drugs are problematic due to the plethora of characteristics that may differ between them. Even head-to-head comparisons in the same study may not determine the optimal target due to differences in pharmacokinetics between the agents. Therefore, the answer to this question relies on theoretical speculations based on knowledge of some of the factors that seem to have an influence on efficacy and safety. Ultimately, drugs with equal pharmacokinetic characteristics that are administered in equipotent doses may have a similar global effect on coagulation, independent of the inhibitory mechanism. Conversely, the differentiated inhibition of the coagulation protease on vascular receptors may play a greater role for effects that are not traditionally considered as part of hemostasis.
抑制凝血的更好靶点是哪种活化凝血因子。由于不同药物之间可能存在大量不同特征，对不同药物研究进行间接比较存在问题。即使在同一研究中进行直接比较，由于药物之间药代动力学的差异，也可能无法确定最佳靶点。因此，这个问题的答案依赖于基于对一些似乎影响疗效和安全性的因素的了解所做的理论推测。最终，具有相同药代动力学特征且以等效剂量给药的药物，可能对凝血有相似的整体作用，而与抑制机制无关。相反，凝血蛋白酶对血管受体的差异化抑制，可能在那些传统上不被视为止血一部分的效应中发挥更大作用。
