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Argatroban

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https://www.readbyqxmd.com/read/29760293/-safety-of-dual-antiplatelet-therapy-with-argatroban-in-patients-with-acute-ischemic-stroke
#1
Yoshinari Nagakane, Eijirou Tanaka, Shinji Ashida, Yuta Kojima, Shiori Ogura, Keiko Maezono, Yasumasa Yamamoto
To prevent early neurological worsening or recurrence in stroke patients with intracranial arterial stenosis or branch atheromatous disease, aggressive antithrombotic therapy, such as dual antiplatelet therapy (DAPT) with or without anticoagulant therapy, is warranted. Such an aggressive antithrombotic therapy, however, may increase the bleeding risk. We studied the risks of DAPT with the anticoagulant argatroban in patients with acute ischemic stroke or transient ischemic attack (TIA). Between October 2011 and September 2015, 341 patients with stroke or TIA, who received DAPT with argatroban within 48 hours after onset, were retrospectively studied...
May 2018: Brain and Nerve, Shinkei Kenkyū No Shinpo
https://www.readbyqxmd.com/read/29759183/evaluation-of-thrombin-inhibitory-activity-of-catechins-by-online-capillary-electrophoresis-based-immobilized-enzyme-microreactor-and-molecular-docking
#2
Qiao-Qiao Li, Feng-Qing Yang, Yin-Zhen Wang, Zhao-Yu Wu, Zhi-Ning Xia, Hua Chen
An online capillary electrophoresis (CE)-based thrombin (THR) immobilized enzyme microreactor (IMER) method was established to screen THR inhibitors in this study. S-2366 was used as chromogenic substrate for determination of THR activity and other kinetic constants. After continuously run for 50 times, the prepared IMER could still remain 89% of the initial immobilized enzyme activity. The Michaelis-Menten constant (Km ) of immobilized THR was measured as 0.514 mmol/L and the half-maximal inhibitory concentration (IC50 ) and inhibition constant (Ki ) of argatroban on THR were determined as 78...
August 1, 2018: Talanta
https://www.readbyqxmd.com/read/29744595/synthesis-and-biocompatibility-of-an-argatroban-modified-polysulfone-membrane-that-directly-inhibits-thrombosis
#3
Xiao Fu, Jian-Ping Ning
Anticoagulation therapy plays a vital role in the prevention of blood clot formation during hemodialysis and hemofiltration, especially for critical care patients. Here, we synthesized a novel argatroban (Arg)-modified polysulfone (PSf) membrane for anticoagulation. Arg was grafted onto the PSF membrane via chemical modification to increase membrane hydrophilicity. Protein adsorption, coagulation, as well as activation of platelets and complement systems were greatly reduced on the Arg-modified PSf membrane...
May 9, 2018: Journal of Materials Science. Materials in Medicine
https://www.readbyqxmd.com/read/29744232/investigation-of-interactions-between-thrombin-and-ten-phenolic-compounds-by-affinity-capillary-electrophoresis-and-molecular-docking
#4
Qiao-Qiao Li, Yu-Xiu Yang, Jing-Wen Qv, Guang Hu, Yuan-Jia Hu, Zhi-Ning Xia, Feng-Qing Yang
Thrombin plays a vital role in blood coagulation, which is a key process involved in thrombosis by promoting platelet aggregation and converting fibrinogen to form the fibrin clot. In the receptor concept, drugs produce their therapeutic effects via interactions with the targets. Therefore, investigation of interaction between thrombin and small molecules is important to find out the potential thrombin inhibitor. In this study, affinity capillary electrophoresis (ACE) and in silico molecular docking methods were developed to study the interaction between thrombin and ten phenolic compounds ( p -hydroxybenzoic acid, protocatechuic acid, vanillic acid, gallic acid, catechin, epicatechin, dihydroquercetin, naringenin, apigenin, and baicalein)...
2018: Journal of Analytical Methods in Chemistry
https://www.readbyqxmd.com/read/29736294/novel-degradation-products-of-argatroban-isolation-synthesis-and-extensive-characterization-using-nmr-and-lc-pda-ms-q-tof
#5
Vinodh Guvvala, Venkatesan Chidambaram Subramanian, Jaya Shree Anireddy, Mahesh Konda
Forced degradation study of argatroban under conditions of hydrolysis (neutral, acidic and alkaline), oxidation, photolysis and thermal stress, as suggested in the ICH Q1A (R2), was accomplished. The drug showed significant degradation under hydrolysis (acidic, alkaline) and oxidation (peroxide stress) conditions. The drug remained stable under thermal and photolytic stress conditions. In total, seven novel degradation products (DP - 1 to DP - 7) were found under diverse conditions, which were not reported earlier...
April 2018: Journal of Pharmaceutical Analysis
https://www.readbyqxmd.com/read/29707901/argatroban-is-stable-in-citrated-whole-blood-for-24-hours
#6
S Guy, S Kitchen, J J Van Veen
INTRODUCTION: Argatroban is a direct thrombin inhibitor used as an anticoagulant for patients who have Heparin induced thrombocytopenia. Quantification can be performed using a dilute thrombin time or anti-iia assay. Our preferred method is Hemoclot Thrombin Inhibitor Assay (HTI).To the best of our knowledge, no one has published on the stability of plasma argatroban in whole citrated blood at room temperature. METHODS: Forty matched samples obtained from 4 patients receiving argatroban...
April 29, 2018: International Journal of Laboratory Hematology
https://www.readbyqxmd.com/read/29706441/retrospective-analysis-of-argatroban-in-353-patients-with-acute-noncardioembolic-stroke
#7
Hiroaki Oguro, Shingo Mitaki, Hiroyuki Takayoshi, Satoshi Abe, Keiichi Onoda, Shuhei Yamaguchi
BACKGROUND: Argatroban is a thrombin inhibitor agent for acute noncardioembolic ischemic stroke in Japan. We studied the prognosis in patients with acute stroke treated by argatroban in comparison with the control group with ozagrel in our hospital. SUBJECTS AND METHODS: A total of 513 patients with acute noncardioembolic ischemic stroke were enrolled retrospectively from our hospital database. Of all patients with stroke, 353 were administered with argatroban. The other 160 control patients were administered with ozagrel...
April 26, 2018: Journal of Stroke and Cerebrovascular Diseases: the Official Journal of National Stroke Association
https://www.readbyqxmd.com/read/29614521/targeting-coagulase-activity-in-staphylococcus-aureus-bacteraemia-a-randomized-controlled-single-centre-trial-of-staphylothrombin-inhibition
#8
Marijke Peetermans, Laurens Liesenborghs, Kathelijne Peerlinck, Eric Van Wijngaerden, Olivier Gheysens, Karolien E Goffin, Marc F Hoylaerts, Marc Jacquemin, Jan Verhaegen, Willy E Peetermans, Peter Verhamme, Thomas Vanassche
BACKGROUND:   Staphylococcus aureus ( S. aureus ) bacteraemia is frequent and carries a high morbidity and mortality. Coagulases secreted by S. aureus initiate blood coagulation by directly activating prothrombin. This pathogen-activated coagulation is insensitive to most antithrombotic drugs, with the exception of small molecule direct thrombin inhibitors (DTIs). DTIs inhibit the coagulase-prothrombin complex, or staphylothrombin, and improve outcome in preclinical models of S. aureus infection...
April 3, 2018: Thrombosis and Haemostasis
https://www.readbyqxmd.com/read/29605959/heparin-induced-thrombocytopenia-in-infants-after-heart-surgery
#9
Juma N Abdillah, Qinghua Hu, Xuliang Chen, Xing Chen, Wu Zhou, Wanjun Luo, Lingjin Huang
BACKGROUND:  Heparin-induced thrombocytopenia (HIT) in infants is a rare disorder, and the diagnosis and management of HIT still remains challenging. Argatroban is a synthetic direct thrombin inhibitor (DTI) that is widely used for treating HIT. However, little is known about the efficacy of the activated clotting time (ACT) test in monitoring DTI treatment as an alternative to the routinely used activated partial thromboplastin time (aPTT). METHODS:  Between July 2013 and January 2015, four infants were diagnosed with HIT after surgical correction of congenital anomalies...
April 1, 2018: Thoracic and Cardiovascular Surgeon
https://www.readbyqxmd.com/read/29559752/anticoagulation-management-during-first-five-days-of-infant-pediatric-extracorporeal-life-support
#10
Kirk R Bingham, Jeffrey B Riley, Gregory J Schears
Anticoagulation during infant-pediatric extracorporeal life support (ECLS) has been a topic of study for many years, but management of anticoagulation is still only partially understood. Adequate anticoagulation during ECLS is imperative for successful outcomes and understanding the individual variables that play part is crucial for properly implementing anticoagulation management strategies. The purpose of our study was to compare the relationships between the variables of activated partial thromboplastin time (aPTT), activated clotting time, international normalized ratio, bleeding, thrombus formation, kaolin + heparinase thromboelastograph alpha angle, kaolin thromboelastograph reaction time (KTEG R-time), heparin dose rates (HDR), antithrombin (AT), anti-Xa, bivalirudin dose rate, argatroban dose rate, interventions, and transfusions...
March 2018: Journal of Extra-corporeal Technology
https://www.readbyqxmd.com/read/29426286/monitoring-of-argatroban-and-lepirudin-anticoagulation-in-critically-ill-patients-by-conventional-laboratory-parameters-and-rotational-thromboelastometry-a-prospectively-controlled-randomized-double-blind-clinical-trial
#11
Martin Beiderlinden, Patrick Werner, Astrid Bahlmann, Johann Kemper, Tobias Brezina, Maximilian Schäfer, Klaus Görlinger, Holger Seidel, Peter Kienbaum, Tanja A Treschan
BACKGROUND: Argatroban or lepirudin anticoagulation therapy in patients with heparin induced thrombocytopenia (HIT) or HIT suspect is typically monitored using the activated partial thromboplastin time (aPTT). Although aPTT correlates well with plasma levels of argatroban and lepirudin in healthy volunteers, it might not be the method of choice in critically ill patients. However, in-vivo data is lacking for this patient population. Therefore, we studied in vivo whether ROTEM or global clotting times would provide an alternative for monitoring the anticoagulant intensity effects in critically ill patients...
February 9, 2018: BMC Anesthesiology
https://www.readbyqxmd.com/read/29421832/heparin-induced-thrombocytopenia-during-obstetric-hospital-admissions
#12
Deepika Sagaram, Zainab Siddiq, Andrew B Eisenberger, Cande V Ananth, Jason D Wright, Mary E D'Alton, Alexander M Friedman
INTRODUCTION:  The rate of heparin-induced thrombocytopenia (HIT) on a population basis is unknown. The objective of this study was to characterize the risk for HIT during antepartum, delivery, and postpartum hospitalizations in the United States. MATERIALS AND METHODS: A large administrative database was used to determine the risk of HIT in hospitalized obstetric patients who received unfractionated heparin (UFH) or low molecular weight heparin (LMWH). Patients were presumed to have HIT if they were exposed to UFH or LMWH, received a diagnosis of HIT, and were administered a medication for the treatment of HIT including bivalirudin, argatroban, fondaparinux, or lepirudin...
February 8, 2018: American Journal of Perinatology
https://www.readbyqxmd.com/read/29367082/argatroban-dosing-in-obesity
#13
Stephanie Elagizi, Kyle Davis
PURPOSE: Obesity is associated with significant alterations in pharmacokinetic and pharmacodynamic properties. The use of weight based anticoagulants such as argatroban may put obese patients at an increased risk of hemorrhagic events. The purpose of this study was to evaluate argatroban dosing requirements in obese vs non-obese patients. METHODS: This single-center, retrospective cohort study included patients ≥18 years with suspected HIT, treated with argatroban for ≥12 h...
March 2018: Thrombosis Research
https://www.readbyqxmd.com/read/29341135/phenolic-fractions-from-nine-trifolium-species-modulate-the-coagulant-properties-of-blood-plasma-in-vitro-without-cytotoxicity-towards-blood-cells
#14
Joanna Kolodziejczyk-Czepas, Malgorzata Sieradzka, Barbara Moniuszko-Szajwaj, Pawel Nowak, Wiesław Oleszek, Anna Stochmal
OBJECTIVE: The study covers an evaluation of the influence of extracts (1-50 μg/ml), isolated from aerial parts of nine Trifolium L. species (i.e. T. alexandrinum, T. fragiferum, T. hybridum, T. incarnatum, T. pallidum, T. pratense, T. resupinatum var. majus, T. resupinatum var. resupinatum and T. scabrum) on haemostatic properties of blood plasma. METHODS: The clot formation and fibrinolysis assay (CFF), blood clotting times, the extrinsic and intrinsic coagulation pathway-dependent polymerization of plasma fibrin were measured...
January 17, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29335786/anti-inflammatory-and-antiplatelet-effects-of-non-vitamin-k-antagonist-oral-anticoagulants-in-acute-phase-of-ischemic-stroke-patients
#15
Taizen Nakase, Junta Moroi, Tatsuya Ishikawa
BACKGROUND: Recently, non-vitamin K antagonist oral anticoagulants such as direct thrombin and direct factor Xa inhibitors have been prescribed for prevention of embolic stroke. While in Japan, argatroban, also a direct thrombin inhibitor, is available for the treatment of atherothrombotic stroke patients. This study aimed to explore whether there is any differences between direct thrombin and direct factor Xa inhibitors regarding the inhibiting effect against thrombogenesis in the clinical setting of acute ischemic stroke...
January 12, 2018: Clinical and Translational Medicine
https://www.readbyqxmd.com/read/29304263/the-prevalence-of-adverse-ocular-hemorrhagic-events-in-patients-utilizing-oral-anticoagulant-and-antiplatelet-therapy-in-routine-clinical-practice
#16
Dattanand M Sudarshana, Eleni K Konstantinou, Sruthi Arepalli, Fabiana Q Silva, Andrew P Schachat, Justis P Ehlers, Rishi P Singh
BACKGROUND AND OBJECTIVE: Previous literature assessing ocular hemorrhagic complications of anticoagulant/antiplatelet medications in routine clinical practice is limited. This study evaluates the prevalence of spontaneous ocular hemorrhagic events associated with anticoagulation/antiplatelet therapy. PATIENTS AND METHODS: A retrospective study was performed to identify patients taking anticoagulants (rivaroxaban [Xarelto; Janssen Pharmaceuticals, Beerse, Belgium], bivalirudin [Angiomax; The Medicines Company, Parsippany, NJ], lepirudin [Refludan; Bayer HealthCare Pharmaceuticals, Berlin, Germany], dabigatran [Pradaxa; Boehringer Ingelheim, Ingelheim am Rhein, Germany], and argatroban) and antiplatelet agents (clopidogrel [Plavix; Bristol-Myers Squibb, New York City, NY], prasugrel [Effient; Lilly Medical, Indianapolis, IN], and ticagrelor [Brilinta; AstraZeneca, Cambridge, UK]) who presented for an eye examination...
January 1, 2018: Ophthalmic Surgery, Lasers & Imaging Retina
https://www.readbyqxmd.com/read/29206646/argatroban-and-bivalirudin-for-perioperative-anticoagulation-in-cardiac-surgery
#17
REVIEW
Andreas Koster, David Faraoni, Jerrold H Levy
No abstract text is available yet for this article.
February 2018: Anesthesiology
https://www.readbyqxmd.com/read/29196860/role-of-thrombin-in-soluble-thrombomodulin-induced-suppression-of-peripheral-hmgb1-mediated-allodynia-in-mice
#18
Ryuichi Tsujita, Maho Tsubota, Yusuke Hayashi, Haruka Saeki, Fumiko Sekiguchi, Atsufumi Kawabata
High mobility group box 1 (HMGB1), a nuclear protein, once released into the extracellular space under pathological conditions, plays a pronociceptive role in redox-dependent distinct active forms, all-thiol HMGB1 (at-HMGB1) and disulfide HMGB1 (ds-HMGB1), that accelerate nociception through the receptor for advanced glycation endproducts (RAGE) and Toll-like receptor 4 (TLR4), respectively. Thrombomodulin (TM), an endothelial membrane protein, and soluble TM, known as TMα, promote thrombin-mediated activation of protein C and also sequester HMGB1, which might facilitate thrombin degradation of HMGB1...
December 1, 2017: Journal of Neuroimmune Pharmacology: the Official Journal of the Society on NeuroImmune Pharmacology
https://www.readbyqxmd.com/read/29169470/use-of-fondaparinux-off-label-or-approved-anticoagulants-for-management-of-heparin-induced-thrombocytopenia
#19
MULTICENTER STUDY
Marc Schindewolf, Julia Steindl, Jan Beyer-Westendorf, Sebastian Schellong, Pascal Maria Dohmen, Johannes Brachmann, Katharina Madlener, Bernd Pötzsch, Robert Klamroth, Johannes Hankowitz, Norbert Banik, Sonja Eberle, Markus Michael Müller, Stefan Kropff, Edelgard Lindhoff-Last
BACKGROUND: Life-threatening heparin-induced thrombocytopenia (HIT) is treated with the alternative nonheparin anticoagulants argatroban, lepirudin, or danaparoid. Frequently, the pentasaccharide fondaparinux is used off-label. OBJECTIVES: The authors sought to investigate the safety and efficacy of the different anticoagulants for treating HIT. METHODS: In a national, multicenter registry study, hospitalized patients who were diagnosed with HIT, an at least intermediate clinical HIT-risk (4Ts score ≥4 points), and received treatment with ≥1 dose of the aforementioned anticoagulants were included...
November 28, 2017: Journal of the American College of Cardiology
https://www.readbyqxmd.com/read/29164814/detection-of-subclinical-arthritis-in-mice-by-a-thrombin-receptor-derived-imaging-agent
#20
Beth Friedman, Michael A Whitney, Elamprakash N Savariar, Christa Caneda, Paul Steinbach, Qing Xiong, Dina V Hingorani, Jessica Crisp, Stephen R Adams, Michael Kenner, Csilla N Lippert, Quyen T Nguyen, Monica Guma, Roger Y Tsien, Maripat Corr
OBJECTIVE: Functional imaging of synovitis could improve both early detection of rheumatoid arthritis (RA) and long-term outcomes. Given the intersection of inflammation with coagulation protease activation, this study was undertaken to examine coagulation protease activities in arthritic mice with a dual-fluorescence ratiometric activatable cell-penetrating peptide (RACPP) that has a linker, norleucine (Nle)-TPRSFL, with a cleavage site for thrombin. METHODS: K/BxN-transgenic mice with chronic arthritis and mice with day 1 passive serum-transfer arthritis were imaged in vivo for Cy5:Cy7 emission ratiometric fluorescence from proteolytic cleavage and activation of RACPPNleTPRSFL ...
January 2018: Arthritis & Rheumatology
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