Department of Neurology and Stroke, Hertie Institute for Clinical Brain Research, University of Tübingen, Tübingen, Germany.
Department of Internal Medicine and Cardiology, Charité University Medicine Berlin - Campus Virchow Klinikum, Berlin, Germany.
Thromb Haemost. 2017 Dec;117(12):2369-2375. doi: 10.1160/TH17-04-0280. Epub 2017 Dec 6.
Background Direct oral anticoagulants (DOACs) are increasingly replacing vitamin K antagonists (VKA) for clinical indications requiring long-term oral anticoagulation. In contrast to VKA, treatment with DOAC including dabigatran—the only direct thrombin inhibitor amongst them—does not require therapeutic drug monitoring. However, in case of treatment complications (e.g., major haemorrhage) and conditions requiring urgent surgery or thrombolytic therapy, information about actual DOAC plasma levels is needed to guide treatment decisions. Due to short reagent stability, limited accuracy at low dabigatran levels and high heparin sensitivity, the applicability of the widely used Hemoclot thrombin inhibitor (HTI) coagulation assay is limited in the emergency setting. Methods Dabigatran concentrations of 288 citrated plasma samples taken from 48 dabigatran-treated patients with drug concentrations of up to 300 ng/mL were measured with the chromogenic anti-IIa Biophen direct thrombin inhibitor (BDTI) assay and results compared with HTI using ultra performance liquid chromatography—tandem mass spectrometry as the reference method for measuring dabigatran plasma concentrations. Results BDTI results showed a very strong correlation with dabigatran concentrations (r = 0.965, p < 0.0001) as well as a low intra- and inter-assay variation of <5%. Compared with HTI, BDTI provides an improved on-board reagent stability of 72 hours, rapid turnaround times comparable to routine coagulation assays, high accuracy at low drug levels and reduced heparin sensitivity. Conclusion The BDTI is an ideal coagulation assay for the around-the-clock determination of dabigatran plasma levels in clinical routine including emergency situations.
直接口服抗凝剂(DOACs)越来越多地取代维生素 K 拮抗剂(VKA)用于需要长期口服抗凝的临床适应证。与 VKA 不同,包括达比加群(唯一的直接凝血酶抑制剂)在内的 DOAC 治疗不需要治疗药物监测。然而,在出现治疗并发症(如大出血)和需要紧急手术或溶栓治疗的情况下,需要了解实际的 DOAC 血浆水平,以指导治疗决策。由于试剂稳定性差、达比加群水平低时准确性有限以及肝素敏感性高,广泛应用的 Hemoclot 凝血酶抑制剂(HTI)凝血测定在紧急情况下的适用性有限。
用显色抗 IIa 生物素直接凝血酶抑制剂(BDTI)测定法测定 288 份来自 48 例达比加群治疗患者的枸橼酸盐血浆样本的达比加群浓度,这些患者的药物浓度高达 300ng/ml,并与 HTI 进行比较,超高效液相色谱-串联质谱法作为测定达比加群血浆浓度的参考方法。
BDTI 结果与达比加群浓度呈很强的相关性(r=0.965,p<0.0001),且内、日间变异均<5%。与 HTI 相比,BDTI 具有改进的即时试剂稳定性(72 小时)、与常规凝血测定相当的快速周转时间、在低药物水平下的高准确性和降低的肝素敏感性。
BDTI 是一种理想的凝血测定法,可在临床常规中(包括紧急情况下)全天候测定达比加群的血浆水平。