New anticoagulants: how to deal with treatment failure and bleeding complications

Kazmi, Rashid; Lwaleed, Bashir A.

doi:10.1111/j.1365-2125.2011.04060.x

Cited by 57 publications

(57 citation statements)

References 84 publications

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“…These classes of oral anticoagulants do not require therapeutic monitoring, have fewer side effects (especially lower rates of major hemorrhage), and have fewer drug and food interactions than warfarin. [509][510][511][512] The challenge for physicians evaluating and considering treatment options for patients with acute ischemic stroke is determining the anticoagulant effect of these agents and estimating the potential increased risk of hemorrhage after reperfusion strategies are initiated.…”

Section: Patients Taking Direct Thrombin Inhibitors and Direct Factormentioning

confidence: 99%

Guidelines for the Early Management of Patients With Acute Ischemic Stroke

Jauch¹,

Saver²,

Adams³

et al. 2013

Stroke

5,374

1,801

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Background and Purpose-The authors present an overview of the current evidence and management recommendations for evaluation and treatment of adults with acute ischemic stroke. The intended audiences are prehospital care providers, physicians, allied health professionals, and hospital administrators responsible for the care of acute ischemic stroke patients within the first 48 hours from stroke onset. These guidelines supersede the prior 2007 guidelines and 2009 updates. Methods-Members of the writing committee were appointed by the American Stroke Association Stroke Council's Scientific Statement Oversight Committee, representing various areas of medical expertise. Strict adherence to the American Heart Association conflict of interest policy was maintained throughout the consensus process. Panel members were assigned topics relevant to their areas of expertise, reviewed the stroke literature with emphasis on publications since the prior guidelines, and drafted recommendations in accordance with the American Heart Association Stroke Council's Level of Evidence grading algorithm. Results-The goal of these guidelines is to limit the morbidity and mortality associated with stroke. The guidelines support the overarching concept of stroke systems of care and detail aspects of stroke care from patient recognition; emergency medical services activation, transport, and triage; through the initial hours in the emergency department and stroke unit. The guideline discusses early stroke evaluation and general medical care, as well as ischemic stroke, specific interventions such as reperfusion strategies, and general physiological optimization for cerebral resuscitation. The American Heart Association makes every effort to avoid any actual or potential conflicts of interest that may arise as a result of an outside relationship or a personal, professional, or business interest of a member of the writing panel. Specifically, all members of the writing group are required to complete and submit a Disclosure Questionnaire showing all such relationships that might be perceived as real or potential conflicts of interest. Guidelines for the Early Management of PatientsThis statement was approved by the American Heart Association Science Advisory and Coordinating Committee on December 12, 2012. A copy of the document is available at http://my.americanheart.org/statements by selecting either the "By Topic" link or the "By Publication Date" link. To purchase additional reprints, call 843-216-2533 or e-mail kelle.ramsay@wolterskluwer.com.The Executive Summary is available as an online-only Data Supplement with this article at http://stroke.ahajournals.org/lookup/suppl/ doi:10.1161/STR.0b013e318284056a/-/DC1.The American Heart Association requests that this document be cited as follows: Jauch EC, Saver JL, Adams HP Jr, Bruno A, Connors JJ, Demaerschalk BM, Khatri P, McMullan PW Jr, Qureshi AI, Rosenfield K, Scott PA, Summers DR, Wang DZ, Wintermark M, Yonas H; on behalf of the American Heart Association Stroke Council, Council on Cardio...

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Section: Patients Taking Direct Thrombin Inhibitors and Direct Factormentioning

confidence: 99%

Guidelines for the Early Management of Patients With Acute Ischemic Stroke

Jauch¹,

Saver²,

Adams³

et al. 2013

Stroke

5,374

1,801

View full text Add to dashboard Cite

show abstract

“…Recent studies on clinical assessment of novel anticoagulants impacts on patients report that PT assays are insensitive or little affected by direct thrombin inhibitors such as dabigatran. 55,56 However, PT is a useful test to access with greater sensitivity the coagulation status in patients receiving FXa inhibitors, such as rivaroxaban or apixaban, which have a linear dose-response behavior . Anticoagulant activity screening assays for all 4,5-dihydro-1H-imidazolyl pyrazoles derivatives (5a-g) in human pooled plasma (n = 6).…”

Section: Coagulation Assaysmentioning

confidence: 99%

Pyrazolyl-Tetrazoles and Imidazolyl-Pyrazoles as Potential Anticoagulants and their Integrated Multiplex Analysis Virtual Screening

Lourenço

Vegi

Faria

et al. 2018

J. Braz. Chem. Soc.

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This article reports a novel virtual screening algorithm seeking the rational identification of novel lead anticoagulants. Seven 5-(3-methyl-1-aryl-1H-pyrazol-4-yl)-1H-tetrazoles and seven novel 1-aryl-4-(4,5-dihydro-1H-imidazol-2-yl)-3-methyl-1H-pyrazoles were obtained in three steps starting from arylhydrazine hydrochlorides as raw materials in good yields: 50-72% and 50-85%, respectively. All compounds were submitted to an in silico target-base pipeline named integrated multiplex analysis virtual screening (IMA-VS), which comprises the evaluation of their (i) fitting physicochemical properties to the chemical environment of the target enzyme; (ii) active-site homing electrostatic potential to the target enzyme; (iii) structural fitting to the target active site through molecular docking; and (iv) overall absorption, distribution, metabolism, excretion and toxicity (ADMET) profile. After the virtual selection of potential anticoagulant hits, all molecules were synthesized and candidates were evaluated in vitro for their anticoagulant and hemolytic profile. The most promising candidate pointed out by IMA-VS was compound 1-(3',4'-dichlorophenyl)-4-(4,5-dihydro-1H-imidazol-2-yl)-3-methyl-1H-pyrazole that shown to display factor Xa (FXa)-specific inhibitory activity in vitro, acting as an uncompetitive inhibitor with an inhibition constant (Ki) = 61.16 ± 12.96 µM, in addition to the lowest hemolytic activity of the series. Further experiments revealed the antithrombotic activity of this compound in an in vivo model of arterial thrombosis induced by FeCl 3 .

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“…Obwohl es gegenwärtig keine klinischen Studien zum Einsatz von rekombinantem aktiviertem Faktor VII (rFVIIa) gibt, kann die Gabe von rFVIIa bei vital bedrohlichen Blutungen in Betracht gezogen werden. Eine spezifische Dosisempfehlung gibt es gegenwärtig nicht; Dosisempfehlungen zur Therapie von Blutungen durch parenterale Antikoagulanzien liegen zwischen 20 und 120 µg/kgKG [10]. Weiterhin werden die Gabe von PPSB, die Faktor II, VII, IX und X enthalten [17], sowie die Gabe von aktivierten PPSB diskutiert [10].…”

Section: Patienten Unter Therapie Mit Neuen Oralen Antikoagulanzien Vunclassified

Neue Antithrombotika

Heidinger

Kemkes‐Matthes

2011

Med Klin

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Vitamin K antagonists and heparins have been standard anticoagulation drugs over the past decades. They are effective and safe but they have several drawbacks which has led to the development of new oral anticoagulants. Dabigatran etexilate is a specific oral thrombin inhibitor and rivaroxaban and apixaban are oral inhibitors of factor Xa. These agents produce a predictable anticoagulant response after fixed-dose administration so that routine coagulation monitoring is unnecessary. Currently, dabigatran etexilate, rivaroxaban and apixaban are licensed for thromboprophylaxis after elective total hip or knee replacement surgery. Since august 2011, dabigatran etexilate is licensed for patients with atrial fibrillation, rivaroxaban will follow. However, indications will be expanded e.g. for therapy of venous thromboembolism. It is important to be aware of the pharmacokinetic and pharmacodynamic profiles of these new agents. The drugs considerably influence the global test of coagulation thus making an interpretation of test results difficult. Currently, there is a lack of suitable coagulation tests to monitor anticoagulation in emergency cases, such as bleeding. Specific antidotes are not yet available.

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New anticoagulants: how to deal with treatment failure and bleeding complications

Cited by 57 publications

References 84 publications

Guidelines for the Early Management of Patients With Acute Ischemic Stroke

Guidelines for the Early Management of Patients With Acute Ischemic Stroke

Pyrazolyl-Tetrazoles and Imidazolyl-Pyrazoles as Potential Anticoagulants and their Integrated Multiplex Analysis Virtual Screening

Neue Antithrombotika

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