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C F Munson, A J Reid
Novel oral anticoagulants (NOACs) have emerged as a good alternative to warfarin in the prevention of stroke for patients with atrial fibrillation. NOAC use is increasing rapidly; therefore, greater understanding of their use in the perioperative period is important for optimal care. Studies and reviews that reported on the use of NOACs were identified, with particular focus on the perioperative period. PubMed was searched for relevant articles published between January 2000 and August 2015. The inevitable rise in the use of NOACs such as rivaroxaban (Xarelto™), apixaban (Eliquis™), edoxaban (Lixiana™) and dabigatran (Pradaxa™) may present a simplified approach to perioperative anticoagulant management due to fewer drug interactions, rapidity of onset of action and relatively short half-lives...
May 2016: Journal of Plastic, Reconstructive & Aesthetic Surgery: JPRAS
(no author information available yet)
Not more effective than warfarin. The lower incidence of bleeding observed among patients selected for these trials must be weighed against the lack of either an antidote or a routine clotting test.
September 2015: Prescrire International
Guyan Liang, J Phillip Bowen
There has been a revolution in the development of effective, small-molecule anticoagulants and antiplatelet agents. Numerous trypsin-like serine proteases have been under active pursuit as therapeutic targets. Important examples include thrombin, factor VIIa, factor Xa, and β-tryptase with indications ranging from thrombosis and inflammation to asthma and chronic obstructive pulmonary disease (COPD). Trypsin-like serine proteases exhibit a highly similar tertiary folding pattern, especially for the region near the substrate binding pocket that includes the conserved catalytic triad consisting of histidine 57, aspartic acid 102, and serine 195...
2016: Current Topics in Medicinal Chemistry
Henry A Spiller, James B Mowry, Alfred Aleguas, Jill R K Griffith, Robert Goetz, Mark L Ryan, Stacey Bangh, Wendy Klein-Schwartz, Scott Schaeffer, Marcel J Casavant
STUDY OBJECTIVE: Rivaroxaban and apixaban are part of a new group of oral anticoagulants targeting factor Xa and approved by the Food and Drug Administration in 2011 and 2012. These oral anticoagulants are administered at fixed daily doses, without the need for laboratory-guided adjustments. There are limited data available on supratherapeutic doses or overdose of the oral Xa inhibitors. This study characterizes the clinical effect in patients exposed to rivaroxaban and apixaban. METHODS: A retrospective study collected data from 8 regional poison centers covering 9 states...
February 2016: Annals of Emergency Medicine
Antonio Gómez-Outes, Ma Luisa Suárez-Gea, Ramón Lecumberri, Ana Isabel Terleira-Fernández, Emilio Vargas-Castrillón
In recent years, several direct-acting oral anticoagulants (DOAC) have become available for use in Europe and other regions in indications related to prophylaxis and treatment of venous and arterial thromboembolism. They include the oral direct thrombin inhibitor dabigatran etexilate (Pradaxa, Boehringer Ingelheim) and the oral direct FXa inhibitors rivaroxaban (Xarelto, Bayer HealthCare), apixaban (Eliquis, Bristol-Myers Squibb), and edoxaban (Lixiana/Savaysa, Daiichi-Sankyo). The new compounds have a predictable dose response and few drug-drug interactions (unlike vitamin k antagonists), and they do not require parenteral administration (unlike heparins)...
November 2015: European Journal of Haematology
Naiyu Zheng, Long Yuan, Qin C Ji, Heidi Mangus, Yan Song, Charles Frost, Jianing Zeng, Anne-Françoise Aubry, Mark E Arnold
Apixaban (Eliquis™) was developed by Bristol-Myers Squibb (BMS) and Pfizer to use as an antithrombotic/anticoagulant agent and has been recently approved for the prevention of stroke and systemic embolism in patients with nonvalvular atrial fibrillation. A clinical study of apixaban, sponsored by BMS and Pfizer, included a pilot exploratory portion to evaluate the potential for future drug concentration monitoring using dried blood spot (DBS) sample collection. For DBS sample collection, a fixed blood volume was dispensed onto a DBS card by either regular volumetric pipette (venous blood collection) or capillary dispenser (finger prick blood collection)...
April 15, 2015: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
Brandon J McMahon, Hau C Kwaan
One of the major advances in the management of thrombosis is arguably the introduction of the new non-vitamin K antagonist oral anticoagulants (NOACs). These are small molecules, designed to directly inhibit specific steps in the coagulation pathway, with dabigatran (Pradaxa), inhibiting thrombin and rivaroxaban (Xarelto), apixiban (Eliquis), edoxaban (Lixiana), and betrixaban being factor Xa inhibitors. They have several advantages over vitamin K antagonists such as warfarin, with more predictable bioavailability, fewer drug interactions, and improved safety, especially intracranial hemorrhage...
March 2015: Seminars in Thrombosis and Hemostasis
Debora Karetová, Jan Bultas
Thromboembolic disease (TD) is a relatively common disease with acute risk of death and potential long-term consequences in term of postthrombotic syndrome or chronic pulmonary hypertension. Anticoagulant therapy is the basic therapeutic procedure; thrombolytic therapy and the introduction cava filter are appropriately indicated for individual cases. In past few years, new direct oral anticoagulant drugs (NOAC) have occurred - Xa factor or thrombin inhibitors which have demonstrated the same efficacy and even higher safety in comparison to conventional treatment...
November 2014: Vnitr̆ní Lékar̆ství
Janice Pursley, Jim X Shen, Alan Schuster, Oanh T Dang, Jim Lehman, Michael H Buonarati, Yan Song, Anne-Francoise Aubry, Mark E Arnold
BACKGROUND: apixaban (BMS-562247) (Eliquis(®)) is a novel, orally active, selective, direct, reversible inhibitor of the coagulation factor Xa (FXa). A sensitive and reliable method was developed and validated for the measurement of apixaban (BMS-562247) and its major circulating metabolite (BMS-730823) in human citrated plasma for use in clinical testing. METHODOLOGY/RESULTS: A 0.100 ml portion of citrated plasma sample was extracted and analyzed by LC-MS/MS. Run times were approximately 3 min...
August 2014: Bioanalysis
Anna Schlüter, Alf Lamprecht
Anticoagulant therapy is widely used for the treatment and prophylaxis of deep vein thrombosis and coronary syndromes. Until now, drugs such as unfractionated heparin and low molecular weight heparins need to be administered parenterally. Parenteral administration results in lower patient compliance compared to oral therapy and for this reason, the focus of various research groups is to develop an oral heparin formulation which is as effective as the parenteral formulation, easy to use and non-toxic. In the last few years, some new oral anticoagulants like Rivaroxaban (Xarelto(®)), Apixaban (Eliquis(®)) and Dabigatranetexilat (Pradaxa(®)) have reached the market, but their use is limited to certain indications...
2014: Current Pharmaceutical Biotechnology
Claire Curtin, Jamie M Hayes, Jeremy Hayes
UNLABELLED: As dental professionals, we should all be familiar with the most common oral anticoagulant, warfarin, and how to manage our patients that are taking it. However, several new oral anticoagulants which have recently been approved by the National Institute for Health and Care Excellence (NICE) are now being prescribed for patients in the United Kingdom. These new oral anticoagulants fall into two different categories: a direct thrombin inhibitor dabigatran etexilate (Pradaxa Boehringer-Ingelheim, Bracknell, Berkshire) and activated Factor X inhibitors rivaroxaban (Xarelto Bayer HealthCare, Newbury, Berkshire) and apixaban (Eliquis Bristol-Myers Squibb, Uxbridge, Middlesex)...
July 2014: Dental Update
Michael J Orwat, Jennifer X Qiao, Kan He, Alan R Rendina, Joseph M Luettgen, Karen A Rossi, Baomin Xin, Robert M Knabb, Ruth R Wexler, Patrick Y S Lam, Donald J P Pinto
In an effort to identify a potential back-up to apixaban (Eliquis®), we explored a series of diversified P4 moieties. Several analogs with substituted gem-dimethyl moieties replacing the terminal lactam of apixaban were identified which demonstrated potent FXa binding affinity (FXa Ki), good human plasma anticoagulant activity (PT EC2x), cell permeability, and oral bioavailability.
August 1, 2014: Bioorganic & Medicinal Chemistry Letters
Robert A Beck, William M King
No abstract text is available yet for this article.
April 15, 2014: American Family Physician
A Lai, N Davidson, S W Galloway, J Thachil
BACKGROUND: New oral anticoagulants (NOACs) offer an alternative to warfarin for preventing stroke in patients with atrial fibrillation. NOACs are expected to replace warfarin and other vitamin K antagonists for most of their indications in the future. Knowledge of the use of NOACs in the perioperative period is important for optimal care. METHODS: Studies that reported on the use of NOACs were identified, focusing on evidence-based guidance relating to the perioperative period...
June 2014: British Journal of Surgery
C Fenger-Eriksen, A-M Münster, E L Grove
New oral anticoagulants like the direct thrombin inhibitor, dabigatran (Pradaxa®), and factor Xa-inhibitors, rivaroxaban (Xarelto®) and apixaban (Eliquis®) are available for prophylaxis and treatment of thromboembolic disease. They are emerging alternatives to warfarin and provide equal or better clinical outcome together with reduced need for routine monitoring. Methods for measuring drug concentrations are available, although a correlation between plasma drug concentrations and the risk of bleeding has not been firmly established...
July 2014: Acta Anaesthesiologica Scandinavica
Christian von Heymann, Lutz Kaufner, Mareike Körber
The new oral anticoagulants directly inhibit either thrombin (Dabigatran, Pradaxa®,) or activated Factor X (rivaroxaban, Xarelto®, and apixaban, Eliquis®) and have been approved for thromboprophylaxis after hip and knee replacement surgery and stroke prevention in non-valvular atrial fibrillation. Moreover, rivaroxaban has been approved for the treatment of deep venous thrombosis, prevention of pulmonary embolism and anticoagulation after acute myocardial infarction. The direct FXa-inhibitor edoxaban (Lixiana®) expects approval for the prevention of stroke in atrial fibrillation in Germany in 2014...
March 2014: Anästhesiologie, Intensivmedizin, Notfallmedizin, Schmerztherapie: AINS
Hira Shafeeq, Tran H Tran
Atrial fibrillation (AF) is the most common cardiac arrhythmia in the U.S. Anticoagulation is recommended for stroke prevention in AF patients with intermediate-to-high stroke risk (i.e., patients with a CHADS2 score of 1 or greater). Warfarin was previously the only option for oral anticoagulation in these patients, but three new oral anticoagulants have become available as alternatives for warfarin in patients with nonvalvular AF. The advantages of the newer agents include a rapid onset, predictable pharmacokinetics, and no need for routine anticoagulation monitoring...
January 2014: P & T: a Peer-reviewed Journal for Formulary Management
Gilles Pernod
The new direct oral anticoagulants directly targeting thrombin (factor IIa) or factor-Xa, are currently used for the treatment of deep venous thrombosis and pulmonary embolism (rivaroxaban, Xarelto) or for the prevention of systemic embolism in non-valvular atrial fibrillation (rivaroxaban; dabigatran, Pradaxa; Apixaban, Eliquis). Given their ease of use, it is expected that these drugs would be widely used in such long-term indications. Beyond their effectiveness, these treatments remain anticoagulant drugs, potentially responsible for bleeding complications, and specific measures should be defined in case of occurrence of such complications...
February 5, 2014: Revue Médicale Suisse
Marine Gegu, Pascal Chevalet, François-Xavier Piloquet, Gilles Berrut, Laure De Decker
Treatment with vitamin K antagonists are subject to a common iatrogenic mainly characterized by hemorrhagic stroke. Their narrow therapeutic range associated with variability largely explains this phenomenon. New oral anticoagulants (NOAC) are now available. dabigatran (Pradaxa®) is a direct and specific thrombin inhibitor. It is excreted mainly by the kidney and is the only which can be dialyzed. Rivaroxaban (Xarelto®) and apixaban (Eliquis®) are factor X activated direct inhibitors. They are highly bound to plasma proteins and are metabolized mainly by the liver, via CYP3A4...
December 2013: Gériatrie et Psychologie Neuropsychiatrie du Vieillissement
(no author information available yet)
In October 2011, DTB reviewed the use of dabigatran, the first new oral anticoagulant licensed for the prevention of stroke and systemic embolism in adult patients with non-valvular atrial fibrillation (AF) and one or more defined risk factors.1 We noted that the potential advantages of dabigatran for many patients with AF and the continuing need to provide warfarin therapy for others, provided an important challenge for the NHS. The use of dabigatran has increased significantly in the UK and two other drugs have been licensed for this indication (▾apixaban-Eliquis, Bristol-Myers Squibb/Pfizer; ▾rivaroxaban-Xarelto, Bayer plc)...
January 2014: Drug and Therapeutics Bulletin
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