Clinical Pharmacology, Medical Faculty of Medicine Mannheim, Ruprecht-Karls-University Heidelberg, Heidelberg, Germany.
Thromb J. 2013 Aug 1;11(1):15. doi: 10.1186/1477-9560-11-15.
New oral anticoagulants (NOAC) are approved for several indications for prophylaxis and treatment of venous thromboembolism and for prevention of embolism in atrial fibrillation at fixed daily doses without need of laboratory guided dose adjustment. Due to their low molecular weight of about 500 to 600 Dalton and their hydrophilicity free anticoagulant is excreted immediately through glomerular filtration into the urine. Impairment of renal function may increase the plasma concentration of the anticoagulants and lowered creatinine clearance is a declared contraindication. In contrast to the initial aim of development the anticoagulant effect is required to be determined in special clinical situations. Several specific and non-specific assays using plasma samples are currently undergoing standardization. As all NOACs are excreted into the urine, specific assays were developed for this matrix to determine them quantitatively of qualitatively. Urine samples can be easily and repetitively obtained avoiding problems and risks associated with blood sampling. The qualitative assay can be performed as a point of care test (POC) also by the patient by judging the different colours for the absence or presence of the drugs with the naked eye. The test is rapid (results available within 15 min), sensitive, specific and accurate and does not require a purified NOAC as control. The tests may be a tool for clinicians who need to know for treatment decisions if a NOAC is on board or not. As the tests are specific for oral direct thrombin inhibitors and for oral direct factor Xa inhibitors, the indication does not interfere with other qualitative POC test in development using clotting systems. The test may be indicated for patients at acute hospitalization, before surgery or central nervous system puncture anaesthesia, if fibrinolytic therapy is indicated, acute deterioration of renal function, and for control of adherence to therapy.
新型口服抗凝剂（NOAC）已被批准用于多种适应证，包括预防和治疗静脉血栓栓塞症，以及预防心房颤动中的栓塞，这些药物均采用固定的日剂量，无需实验室指导剂量调整。由于其分子量约为 500 至 600 道尔顿，且具有亲水性，因此无抗凝活性的药物会立即通过肾小球滤过进入尿液中排泄。肾功能损害可能会增加抗凝剂的血浆浓度，而降低的肌酐清除率是明确的禁忌证。与最初的开发目标相反，需要在特殊临床情况下确定抗凝剂的作用。目前正在对几种使用血浆样本的特异性和非特异性检测方法进行标准化。由于所有的 NOAC 都被排泄到尿液中，因此针对该基质开发了特异性检测方法，以定量或定性地确定它们。尿液样本易于获得且可重复，可避免与采血相关的问题和风险。定性检测可作为即时护理检测（POC）由患者进行，通过肉眼判断药物缺失或存在的不同颜色来进行。该检测快速（15 分钟内即可获得结果）、灵敏、特异且准确，且不需要纯化的 NOAC 作为对照。对于需要了解是否使用了 NOAC 的治疗决策的临床医生来说，这些检测可能是一种工具。由于这些检测方法特异性针对口服直接凝血酶抑制剂和口服直接因子 Xa 抑制剂，因此该适应证不会干扰使用凝血系统开发的其他即时护理 POC 检测。如果需要进行纤维蛋白溶解治疗、肾功能急性恶化、或需要控制治疗依从性，那么这些检测可能适用于急性住院、手术前或中枢神经系统穿刺麻醉的患者。
