Direct oral anticoagulants (DOACs): From the laboratory point of view.

IF 2.1 4区 医学 Q3 PHARMACOLOGY & PHARMACY Acta Pharmaceutica Pub Date : 2022-12-01 DOI:10.2478/acph-2022-0034
Sandra Margetić, Sandra Šupraha Goreta, Ivana Ćelap, Marija Razum
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引用次数: 1

Abstract

Direct oral anticoagulants (DOACs) represent a new generation of drugs that have been increasingly used in the prevention and treatment of thromboembolic states. According to the mechanism of anticoagulant action, DOACs are divided into two groups: direct inhibitors of thrombin (dabigatran) and direct inhibitors of activated factor X (FXa) (rivaroxaban, apixaban, edoxaban, betrixaban). Compared to the vitamin K antagonists, DOACs are superior in terms of onset of action, pharmacokinetic and pharmacodynamics properties and fixed daily dose without the need for routine coagulation monitoring. Despite these advantages, there are clinical conditions in which laboratory measurement of DOACs should be performed. Although DOACs have an impact on screening haemostasis assays (prothrombin time, PT; activated partial thromboplastin time, aPTT; and thrombin time, TT), these tests are not appropriate for quantifying drug levels. Therefore, specific quantitative methods (LC-MS/MS as a gold standard method for all DOACs, coagulometric and chromogenic assays for dabigatran, and chromogenic anti-Xa assays with drug-specific calibrators for inhibitors of FXa) should only be used for determination of DOACs concentration. The aim of this review is to present all aspects of laboratory assessment of DOACs, including pre-analytical, analytical and post-analytical factors in the overall testing process with a special accent on the available specific quantitative methods for measurement of DOACs in circulation.

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直接口服抗凝剂(DOACs):从实验室的角度来看。
直接口服抗凝剂(DOACs)代表了新一代药物,已越来越多地用于预防和治疗血栓栓塞状态。根据抗凝作用机制,doac分为凝血酶直接抑制剂(达比加群)和活化因子X直接抑制剂(FXa)(利伐沙班、阿哌沙班、依多沙班、倍曲沙班)两组。与维生素K拮抗剂相比,DOACs在起效、药代动力学和药效学特性以及固定日剂量方面具有优势,无需常规凝血监测。尽管有这些优点,但仍有临床条件需要进行doac的实验室测量。虽然DOACs对筛选止血试验有影响(凝血酶原时间,PT;活化部分凝血活素时间(aPTT);和凝血酶时间,TT),这些试验不适合定量药物水平。因此,特定的定量方法(LC-MS/MS作为所有DOACs的金标准方法,达比加群的凝固测定和显色测定,以及FXa抑制剂的药物特异性校定剂显色抗xa测定)只能用于DOACs浓度的测定。本综述的目的是介绍doac实验室评估的所有方面,包括整个测试过程中的分析前,分析和分析后因素,并特别强调用于测量流通中doac的可用具体定量方法。
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来源期刊
Acta Pharmaceutica
Acta Pharmaceutica PHARMACOLOGY & PHARMACY-
CiteScore
5.20
自引率
3.60%
发文量
20
审稿时长
>12 weeks
期刊介绍: AP is an international, multidisciplinary journal devoted to pharmaceutical and allied sciences and contains articles predominantly on core biomedical and health subjects. The aim of AP is to increase the impact of pharmaceutical research in academia, industry and laboratories. With strong emphasis on quality and originality, AP publishes reports from the discovery of a drug up to clinical practice. Topics covered are: analytics, biochemistry, biopharmaceutics, biotechnology, cell biology, cell cultures, clinical pharmacy, drug design, drug delivery, drug disposition, drug stability, gene technology, medicine (including diagnostics and therapy), medicinal chemistry, metabolism, molecular modeling, pharmacology (clinical and animal), peptide and protein chemistry, pharmacognosy, pharmacoepidemiology, pharmacoeconomics, pharmacodynamics and pharmacokinetics, protein design, radiopharmaceuticals, and toxicology.
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