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Novel anticoagulants

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https://www.readbyqxmd.com/read/28454485/cheminformatics-based-anticoagulant-study-of-traditionally-used-medicinal-plants
#1
Mahdi Alikhani Pour, Soroush Sardari, Ali Eslamifar, Abid Azhar, Mohammad Rezvani, Milad Nazari
Backgroung: Medicinal plants, as a complementary medicine, have been used to treat various diseases since ancient times. These plants have numerous beneficial applications and are the source of certain conventional drugs. In diseases such as stroke and ischemia, which are caused by several factors, abnormal coagulation is an important causative factor. Accordingly, novel and effective therapies such as herbal remedies should be practiced to prevent such lethal diseases. Methods: Using the available databases such as Google Scholar and PubMed, the previously reported anticoagulant compounds and plants possessing anticoagulant activity were identified and collected in two separate lists...
April 29, 2017: Iranian Biomedical Journal
https://www.readbyqxmd.com/read/28439617/-stroke-prophylaxis-in-atrial-fibrillation-when-how-and-for-whom
#2
T Maurer, C Sohns
In patients suffering from atrial fibrillation (AF), modern antithrombotic therapy and anticoagulation strategies should be individualized based on shared decision making including patient preferences and the absolute and relative risks of stroke and bleeding. Estimation of the individual risk for stroke is still based on the CHA2DS2-VASc score. Based on the most recent guidelines for the management of AF, oral anticoagulation therapy should be considered for men with a CHA2DS2-VASc score ≥1 and women with a score ≥2, balancing the expected stroke reduction, risk of bleeding and patient preference...
April 24, 2017: Herz
https://www.readbyqxmd.com/read/28431413/novel-oral-anticoagulants-and-trauma-the-results-of-a-prospective-american-association-for-the-surgery-of-trauma-multi-institutional-trial
#3
Leslie Kobayashi, Galinos Barmparas, Patrick Bosarge, Carlos V Brown, Marko Bukur, Matthew M Carrick, Richard D Catalano, Jan Holly-Nicolas, Kenji Inaba, Stephen Kaminski, Amanda L Klein, Tammy Kopelman, Eric J Ley, Ericca M Martinez, Forrest O Moore, Jason Murry, Raminder Nirula, Douglas Paul, Jacob Quick, Omar Rivera, Martin Schreiber, Raul Coimbra
BACKGROUND: The number of anticoagulated trauma patients is increasing. Trauma patients on warfarin have been found to have poor outcomes, particularly after intracranial hemorrhage (ICH). However, the effect of novel oral anticoagulants (NOAs) on trauma outcomes is unknown. We hypothesized that patients on NOAs would have higher rates of ICH, ICH progression, and death compared with patients on traditional anticoagulant and antiplatelet agents. METHODS: This was a prospective observational trial across 16 trauma centers...
May 2017: Journal of Trauma and Acute Care Surgery
https://www.readbyqxmd.com/read/28428567/novel-oral-anticoagulants-and-exodontia-the-evidence
#4
S Nathwani, C Wanis
Background Haemostasis is crucial for the success of oral surgical treatment as bleeding problems can cause complications both pre- and post-operatively. Patients on anticoagulant drugs present a challenge due to their increased risk of bleeding.Aims To review the evidence for the management of oral surgery patients on novel oral anticoagulant therapy.Methods A literature review was conducted in May 2016 of free-text and MESH searches (keywords: apixaban, dabigatran, rivaroxaban and dental extractions) in the Cochrane Library, PubMed and CINAHL...
April 21, 2017: British Dental Journal
https://www.readbyqxmd.com/read/28422079/synthetic-fluororutaecarpine-inhibits-inflammatory-stimuli-and-activates-endothelial-transient-receptor-potential-vanilloid-type-1
#5
Chi-Ming Lee, Jiun-An Gu, Tin-Gan Rau, Chi Wang, Chiao-Han Yen, Shih-Hao Huang, Feng-Yen Lin, Chun-Mao Lin, Sheng-Tung Huang
The natural product, rutaecarpine (RUT), is the main effective component of Evodia rutaecarpa which is a widely used traditional Chinese medicine. It has vasodilation, anticoagulation, and anti-inflammatory activities. However, further therapeutic applications are limited by its cytotoxicity. Thus, a derivative of RUT, 10-fluoro-2-methoxyrutaecarpine (F-RUT), was designed and synthesized that showed no cytotoxicity toward RAW264.7 macrophages at 20 μM. In an anti-inflammation experiment, it inhibited the production of nitric oxide (NO) and tumor necrosis factor (TNF)-α in lipopolysaccharide (LPS)-stimulated RAW264...
April 19, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28421343/antiplatelets-and-anticoagulants-in-vitreoretinal-surgery-with-a-special-emphasis-on-novel-anticoagulants-a-national-survey-and-review
#6
REVIEW
Rupa Patel, Stephen Charles, Assad Jalil
PURPOSE: To survey current practice and opinion regarding the cessation of antiplatelet and anticoagulant agents prior to vitreoretinal surgery, with special emphasis on novel anticoagulants, and to provide an overview of current literature. METHODS: An online survey was sent to 167 members of the British and Eire Association of Vitreoretinal Surgeons (BEAVRS). A literature search and analysis was conducted on studies that reviewed the bleeding risk of antiplatelet and anticoagulant agents...
April 18, 2017: Graefe's Archive for Clinical and Experimental Ophthalmology
https://www.readbyqxmd.com/read/28416977/trends-in-physiological-coagulation-factors-in-japanese-patients-receiving-novel-oral-anticoagulants
#7
Tomoyuki Nagao, Hiroshi Hunakubo, Mayu Suzuki, Takashi Kataoka, Satoshi Okumura, Norihiro Shinoda, Ken Harada, Bunichi Kato, Masataka Kato, Nobuyuki Marui, Shinichi Sakai, Tetsuya Amano, Toyoaki Murohara
BACKGROUND: Little is known about physiological anticoagulation effects via antithrombin III (AT III) and protein C/S (PC/PS) in patients using new oral anticoagulants (NOACs). METHODS: We evaluated 120 consecutive patients with non-valvular atrial fibrillation (AF) receiving NOACs. Patients were randomly divided into three groups: a dabigatran group (DG, N=40), a rivaroxaban group (RG, N=40) or an apixaban group (AG, N=40). A warfarin group (WG, N=40) was matched with NOAC groups for age, sex and type of AF during the same time period...
April 2017: Journal of Arrhythmia
https://www.readbyqxmd.com/read/28415603/synthesis-and-evaluation-of-anthranilamide-based-derivatives-as-fxa-inhibitors
#8
Changjiang Huang, Wenzhi Wang, Yao Li, Shijun Zhang, Fancui Meng, Weiren Xu, Jing Yuan, Ligong Chen
Factor Xa (FXa) plays a significant role in the blood coagulation cascade and is a promising target for anticoagulation drugs. Three oral FXa inhibitors have been approved by FDA for treating thrombotic diseases. In this study, 43 novel compounds were synthesized anthranilamide-based FXa inhibitors aiming to ameliorate the toxicity of traditional FXa inhibitors in clinic. The data indicated that the compounds 6a, 6a-b, 6a-e, 6k, 6k-a and 6k-b showed remarkable FXa inhibitory activity and excellent selectivity over thrombin in vitro...
March 21, 2017: Oncotarget
https://www.readbyqxmd.com/read/28413976/laboratory-monitoring-or-measurement-of-direct-oral-anticoagulants-doacs-advantages-limitations-and-future-challenges
#9
Emmanuel J Favaloro, Leonardo Pasalic, Jennifer Curnow, Giuseppe Lippi
BACKGROUND: The Direct Oral Anticoagulants (DOACs) represent a new generation of antithrombotic agents, providing direct inhibition of either thrombin (factor IIa; FIIa) or activated factor X (FXa). Around the globe, their use is progressively rising, as these new agents replace the historical anticoagulants (heparin and vitamin K antagonists including warfarin) for various clinical conditions in medical practice. Other acronyms used to designate DOACs include TSOAC (target specific oral anticoagulants) and NOAC (novel; or non-vitamin K antagonist oral anticoagulants)...
April 17, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28413504/early-initiation-of-argatroban-therapy-in-the-management-of-acute-superior-mesenteric-venous-thrombosis
#10
Qiu Zeng, Qi-Ning Fu, Feng-He Li, Xue-Hu Wang, Hong Liu, Yu Zhao
Acute superior mesenteric venous thrombosis (ASMVT) is an intractable disease with poor prognosis. Argatroban, a direct thrombin inhibitor, may be a novel anticoagulant method in the therapy of ASMVT. The aim of the present study was to assess the efficacy and safety of early argatroban therapy in ASMVT patients. The current retrospective study reviewed a consecutive series of ASMVT patients receiving early argatroban therapy during hospitalization between March 2013 and April 2014, with 18 ASMVT patients included in the study...
April 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28409645/evaluation-of-platelet-function-in-thrombocytopenia
#11
Mette Tiedemann Skipper, Peter Rubak, Jesper Stentoft, Anne-Mette Hvas, Ole Halfdan Larsen
Whole blood aggregometry is a functional assay for determination of platelet function. Until now, whole blood aggregometry has not been considered feasible at low platelet counts. Hence, the objectives of the present study were to explore platelet function in thrombocytopenia using a novel index of impedance aggregometry adjusted for platelet count and evaluate the association to platelet function assessed by flow cytometry. Hirudin anticoagulated blood was collected from 20 healthy volunteers, 20 patients with primary immune thrombocytopenia (ITP), and 17 hematological cancer patients...
April 14, 2017: Platelets
https://www.readbyqxmd.com/read/28408226/discovery-of-novel-aminobenzisoxazole-derivatives-as-orally-available-factor-ixa-inhibitors
#12
Isao Sakurada, Toshiya Endo, Katsuyoshi Hikita, Tomokazu Hirabayashi, Yoshitaka Hosaka, Yutaka Kato, Yoshitaka Maeda, Shigeki Matsumoto, Takashi Mizuno, Hiroshi Nagasue, Teruyuki Nishimura, Shunsuke Shimada, Mikihiko Shinozaki, Keiko Taguchi, Katsutoshi Takeuchi, Tooru Yokoyama, Alan Hruza, Paul Reichert, Ting Zhang, Harold B Wood, Kazunari Nakao, Shoji Furusako
Using structure based drug design, novel aminobenzisoxazoles as coagulation factor IXa inhibitors were designed and synthesized. Highly selective inhibition of FIXa over FXa was demonstrated. Anticoagulation profile of selected compounds was evaluated by aPTT and PT tests. In vitro ADMET and pharmacokinetic (PK) profiles were also evaluated.
March 6, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28405673/gly74ser-mutation-in-protein-c-causes-thrombosis-due-to-a-defect-in-protein-s-dependent-anticoagulant-function
#13
Changming Chen, Likui Yang, Bruno O Villoutreix, Xuefeng Wang, Qiulan Ding, Alireza R Rezaie
Protein C is a vitamin K-dependent serine protease zymogen in plasma which upon activation by thrombin in complex with thrombomodulin (TM) down-regulates the clotting cascade by a feedback loop inhibition mechanism. Activated protein C (APC) exerts its anticoagulant function through protein S-dependent degradation of factors Va and VIIIa. We recently identified a venous thrombosis patient whose plasma level of protein C antigen is normal, but its anticoagulant activity is only 34 % of the normal level. Genetic analysis revealed that the proband and her younger brother carry a novel heterozygous mutation c...
April 13, 2017: Thrombosis and Haemostasis
https://www.readbyqxmd.com/read/28403626/direct-factor-ixa-inhibition-with-the-rna-aptamer-pegnivacogin-reduces-platelet-reactivity-in-vitro-and-residual-platelet-aggregation-in-patients-with-acute-coronary-syndromes
#14
Dawid L Staudacher, Vera Putz, Lukas Heger, Jochen Reinöhl, Marcus Hortmann, Steven L Zelenkofske, Richard C Becker, Christopher P Rusconi, Christoph Bode, Ingo Ahrens
BACKGROUND: Residual platelet reactivity is a predictor of poor prognosis in patients with acute coronary syndromes (ACSs) undergoing percutaneous coronary intervention. Thrombin is a major platelet activator and upon initiation of the coagulation cascade, it is subsequently produced downstream of factor IXa, which itself is known to be increased in ACS. Pegnivacogin is a novel RNA-aptamer based factor IXa inhibitor featuring a reversal agent, anivamersen. We hypothesized that pegnivacogin could reduce platelet reactivity...
April 1, 2017: European Heart Journal. Acute Cardiovascular Care
https://www.readbyqxmd.com/read/28396618/apixaban-for-the-treatment-of-saphenous-vein-graft-thrombosis-presenting-as-unstable-angina-a-case-report
#15
Makoto Saigan, Tsuyoshi Isawa, Tatsushi Ootomo
BACKGROUND: Saphenous vein graft thrombosis can present as unstable angina. However, percutaneous coronary intervention for saphenous vein graft lesions poses a high risk of slow flow related to the procedure. Here we present the utilization of the novel oral anticoagulant, apixaban, in the treatment of unstable angina with extensive saphenous vein graft thrombus, leading to considerable thrombus resolution and eliminating the need of percutaneous coronary intervention. CASE PRESENTATION: A 72-year-old man with 3-vessel coronary artery bypass graft surgery using a saphenous vein graft and a left internal mammary artery, performed 25 years earlier, presented at our hospital with recurrent chest tightness...
2017: Thrombosis Journal
https://www.readbyqxmd.com/read/28396155/partial-purification-and-identification-of-a-metalloproteinase-with-anticoagulant-activity-from-rhizostoma-pulmo-barrel-jellyfish
#16
Akriti Rastogi, Angshuman Sarkar, Dibakar Chakrabarty
Rhizostoma pulmo (Barrel Jellyfish) is one of the commonly found jellyfishes on the South-Goan coast of India. Here we present characterization of R. pulmo tentacle extract. The tentacle extracts were found to be capable of affecting the hemostatic system at three different levels, as it exhibited fibrinogenolysis, fibrinolysis and inhibition of ADP induced platelet aggregation. It preferentially cleaved the Aα chain of fibrinogen, followed by the Bβ chain and the γ chain. The tentacle extract also showed significant hemolytic activity against human RBCs and strong proteolytic activity for substrates like (azo) casein and gelatin...
June 15, 2017: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/28393726/a-cost-comparison-of-warfarin-vs-enoxaparine-or-new-oral-anticoagulants-used-for-the-treatment-of-patients-with-pulmonary-embolism
#17
Murat Türk, Yağmur Aldağ, İpek Kıvılcım Oğuzülgen, Numan Ekim
Introduction: Recently, novel oral anticoagulants (rivaroxaban, dabigatran, apixaban) have been approved for pulmonary embolism (PE) treatment. Each anticoagulant used during initial and maintenance therapy has direct and indirect costs for healthcare systems. Demonstrating the costs of treatment with different anticoagulants in a specific patient group will be helpful for clinicians determining treatment strategies. Materials and Methods: Retrospective data of 118 patients with PE who were hospitalized and treated with warfarin for at least 3 months were evaluated...
September 2016: Tüberküloz Ve Toraks
https://www.readbyqxmd.com/read/28390065/trends-in-the-prescription-of-novel-oral-anticoagulants-in-uk-primary-care
#18
S Y Loo, S Dell'Aniello, L Huiart, C Renoux
AIMS: Novel oral anticoagulants (NOAC) are alternatives to vitamin-K antagonists (VKA) for the prevention of thromboembolism. It is unclear how NOAC have been adopted in the UK since first introduced in 2008. This study was conducted to describe the trends in the prescription of NOAC, including dabigatran, rivaroxaban, and apixaban. METHODS: Using the UK's Clinical Practice Research Datalink, the rates of new users of NOAC and VKA from 2009 to 2015 were calculated with Poisson regression...
April 7, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28389110/design-synthesis-and-biological-activity-of-novel-tetrahydropyrazolopyridone-derivatives-as-fxa-inhibitors-with-potent-anticoagulant-activity
#19
Xiaoqing Sun, Zexin Hong, Moyi Liu, Su Guo, Di Yang, Yong Wang, Tian Lan, Linyu Gao, Hongxia Qi, Ping Gong, Yajing Liu
A series of novel tetrahydropyrazolopyridone derivatives containing 1,3,4-triazole, triazolylmethyl, and partially saturated heterocyclic moieties as P2 binding element was designed, synthesized, and evaluated in vitro for anticoagulant activity in human and rabbit plasma. All compounds showed moderate to significant potency, and compounds 15b, 15c, 20b, 20c, and 22b were further examined for their inhibitory activity against human FXa in vitro. While compounds 15c and 22b were tested for rat venous thrombosis in vivo...
May 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28382923/a-compliant-and-biomimetic-three-layered-vascular-graft-for-small-blood-vessels
#20
Yi Zhang, Xiangshun Li, Géraldine Guex, Shanshan Liu, Eike Müller, Riccardo Innocenti Malini, Huijing Zhao, Markus Rottmar, Katharina Maniura, Rene Rossi, Fabrizio Spano
Engineering a small diameter vascular graft with mechanical and biological properties comparable to living tissues remains challenging. Often, current devices lead to thrombosis and unsatisfactory long-term patency as a result of poor blood compatibility and a mismatch between the mechanical properties of the living tissue and the implanted biomaterial. Address-ing all these requirements is essential to produce scaffolds able to survive throughout the life of the patient. For this purpose, we fabricated a novel three-layered vascular graft by combining electrospinning and braiding...
April 6, 2017: Biofabrication
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