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https://www.readbyqxmd.com/read/27473419/characterization-of-the-fluorescent-spectra-and-intensity-of-dabigatran-and-dabigatran-etexilate-application-to-hplc-analysis-with-fluorescent-detection
#1
Harvey A Schwertner, John J Stankus
There is considerable interest in dabigatran etexilate (Pradaxa) and its major metabolite, dabigatran, which has been shown to be an important inhibitor of thrombin and clotting. In this study, the fluorescent excitation and emission spectra of dabigatran and dabigatran etexilate were characterized. In addition, a ultra performance liquid chromatography (UPLC) and high performance liquid chromatography (HPLC) method using fluorescent detection was developed for the analysis of dabigatran. Dabigatran and dabigatran etexilate were found to have excitation and emission maxima of 310 and 375 nm and 335 and 400 nm, respectively...
July 29, 2016: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/27396624/a-solid-self-nanoemulsifying-system-of-the-bcs-class-iib-drug-dabigatran-etexilate-to-improve-oral-bioavailability
#2
Fujuan Chai, Linlin Sun, Yafei Ding, Xiaoqing Liu, Yajie Zhang, Thomas J Webster, Chunli Zheng
AIM: To develop dabigatran etexilate (DE)-loaded self-nanoemulsifying drug delivery systems (SNEDDS) for the prevention of stroke and thromboembolism. MATERIALS & METHODS: SNEDDS were optimized by ternary phase diagrams and then further solidified into dispersible tablets. In vitro dissolution was analyzed by a phase distribution study. In situ absorption and in vivo pharmacokinetic studies were tested in male Sprague-Dawley rats. RESULTS: The phase distribution study showed that more than 60% of DE was retained in the oil phase...
July 2016: Nanomedicine
https://www.readbyqxmd.com/read/27388764/idarucizumab-a-review-as-a-reversal-agent-for-dabigatran
#3
Yahiya Y Syed
Idarucizumab (Praxbind(®)), a humanized monoclonal antibody, is a specific reversal agent for the direct oral thrombin inhibitor dabigatran, available as its prodrug dabigatran etexilate (Pradaxa(®)). Idarucizumab is approved in several countries (including the USA, the EU, Canada and Australia) for use in adult patients on dabigatran when the reversal of its anticoagulant effects is required for emergency surgery/procedures or in the event of life-threatening or uncontrolled bleeding. In the ongoing pivotal RE-VERSE AD trial in these populations (n = 90), intravenous idarucizumab 5 g reversed dabigatran-induced prolongation of dilute thrombin time (dTT) and ecarin clotting time (ECT) within minutes...
August 2016: American Journal of Cardiovascular Drugs: Drugs, Devices, and Other Interventions
https://www.readbyqxmd.com/read/27227858/praxbind-available-as-antidote-to-bleeding-from-pradaxa
#4
Diane S Aschenbrenner
No abstract text is available yet for this article.
June 2016: American Journal of Nursing
https://www.readbyqxmd.com/read/27146196/carbon-13-and-carbon-14-labeled-dabigatran-etexilate-and-tritium-labeled-dabigatran
#5
Bachir Latli, Ralf Kiesling, Stefan Aßfalg, Max Chevliakov, Matt Hrapchak, Scot Campbell, Nina Gonnella, Carl A Busacca, Chris H Senanayake
Dabigatran etexilate or pradaxa, a novel oral anticoagulant, is a reversible, competitive, direct thrombin inhibitor. It is used to prevent strokes in patients with atrial fibrillation and the formation of blood clots in the veins (deep venous thrombosis) in adults who have had an operation to replace a hip or a knee. Pradaxa is the only novel oral anticoagulant available with both proven superiority to warfarin and a specific reversal agent for use in rare emergency situations. The detailed description of the synthesis of carbon-13 and carbon-14 labeled dabigatran etexilate, and tritium labeled dabigatran is described...
May 5, 2016: Journal of Labelled Compounds & Radiopharmaceuticals
https://www.readbyqxmd.com/read/27013144/novel-oral-anticoagulants-in-plastic-surgery
#6
REVIEW
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
https://www.readbyqxmd.com/read/26881855/a-novel-coagulation-parameter-monitoring-bleeding-tendency-of-chinese-nonvalvular-atrial-fibrillation-patients-prescribing-dabigatran-etexilate
#7
Hong Wang, Yun Zhou, Guodong Rong, Lin Lu, Jie Zhang
The objective of this study was to find a new parameter to monitor bleeding tendency after dabigatran etexilate (Pradaxa) medication in Chinese nonvalvular atrial fibrillation patients. Blood samples of 231 nonvalvular atrial fibrillation patients were collected and five routine coagulation examinations (prothrombin time/International normalized ratio, activated partial thromboplastin time, fibrinogen assay, thrombin time and D-dimer) were assayed. After dabigatran etexilate administration, prolonged activated partial thromboplastin time and thrombin time were observed, especially TT...
July 2016: Blood Coagulation & Fibrinolysis: An International Journal in Haemostasis and Thrombosis
https://www.readbyqxmd.com/read/26731215/bilateral-spontaneous-hyphema-vitreous-hemorrhage-and-choroidal-detachment-with-concurrent-dabigatran-etexilate-therapy
#8
Kevin Wang, Justis P Ehlers
A 79-year-old woman was referred for rapid onset of painless bilateral vision loss. Anterior segment exams revealed bilateral spontaneous hyphema and fibrin accumulation. Observation of the posterior chamber by B-scan ultrasound showed vitreous hemorrhage and choroidal detachment bilaterally. No evidence of additional intraocular inflammation was present. Laboratory work-up for hematologic abnormalities was unremarkable. These hemorrhagic events were suspected to be a complication from taking the novel anticoagulant, dabigatran etexilate (Pradaxa; Boehringer, Ingelheim, Germany)...
January 2016: Ophthalmic Surgery, Lasers & Imaging Retina
https://www.readbyqxmd.com/read/26681901/pharmaceutical-approval-update
#9
Chris Fellner
Idarucizumab (Praxbind) to reverse the anticoagulant effects of dabigatran (Pradaxa); aripiprazole lauroxil (Aristada) for the treatment of schizophrenia; and insulin degludec injection (Tresiba) for diabetes.
December 2015: P & T: a Peer-reviewed Journal for Formulary Management
https://www.readbyqxmd.com/read/26578027/idarucizumab-first-global-approval
#10
REVIEW
Celeste B Burness
Idarucizumab (Praxbind(®)) is a fully humanized, monoclonal antibody fragment developed by Boehringer Ingelheim as a specific antidote to reverse the anticoagulant effect of the direct oral thrombin inhibitor dabigatran etexilate (Pradaxa(®)). Idarucizumab received its first global approval, in the USA, in October 2015 for use in adult patients treated with dabigatran etexilate when rapid reversal of its anticoagulant effects is required for emergency surgery/urgent procedures or in life-threatening or uncontrolled bleeding...
December 2015: Drugs
https://www.readbyqxmd.com/read/26489812/thrombin-time-and-anti-iia-dabigatran-s-activity-hypothesis-of-thrombin-time-s-predictive-value
#11
Maïlys Le Guyader, Mohammed Kaabar, Pierre Lemaire, Fabienne Pineau Vincent
Dabigatran etexilate (Pradaxa®) is a new oral anticoagulant, competitive inhibitor, selective, fast, direct and reversible of thrombin. Dabigatran has an impact on a large panel of used coagulation tests. There is no relationship between thrombin time's lengthening and anti-IIa activity. This study defines thrombin time's predictive value, when its time is normal. The result of negative value is 97,6%. 255 patients were studied between January 2013 and July 2014. Thrombin time and anti-IIa activity were dosed for each patient...
September 2015: Annales de Biologie Clinique
https://www.readbyqxmd.com/read/26452739/pradaxa-induced-esophageal-ulcer
#12
Michele Wood, Paul Shaw
Pradaxa (dabigatran) is a direct thrombin inhibitor approved for prevention of stroke and systemic embolism in patients with non-valvular atrial fibrillation. We describe a case of esophageal ulceration associated with Pradaxa administration in a 75-year-old man. The patient reported difficulty swallowing and a burning sensation after taking his first dose of Pradaxa. An esophagogastroduodenoscopy (EGD) revealed linear ulcerations in the mid-esophagus. Pradaxa was held beginning the day before the EGD. The patient reported that his pain and difficulty swallowing resolved on stopping Pradaxa...
2015: BMJ Case Reports
https://www.readbyqxmd.com/read/26436165/dabigatran-pradaxa-deep-vein-thrombosis-and-pulmonary-embolism-warfarin-remains-the-standard-drug
#13
(no author information available yet)
Not more effective than warfarin in three "non-inferiority" trials. Less bleeding but more acute coronary events with dabigatran, and still no antidote.
June 2015: Prescrire International
https://www.readbyqxmd.com/read/26405332/epinephrine-for-anaphylaxis-are-you-ready-to-treat-anaphylaxis-don-t-open-pradaxa-capsules-control-new-ropivacaine-minibags
#14
Michael R Cohen, Judy L Smetzer
No abstract text is available yet for this article.
June 2015: Hospital Pharmacy
https://www.readbyqxmd.com/read/26369819/development-of-trypsin-like-serine-protease-inhibitors-as-therapeutic-agents-opportunities-challenges-and-their-unique-structure-based-rationales
#15
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
https://www.readbyqxmd.com/read/26258841/waiting-for-the-antidote-the-journey-of-idarucizumab-as-a-potential-specific-reversal-agent-for-dabigatran-pradaxa
#16
(no author information available yet)
No abstract text is available yet for this article.
September 2015: Clinical Nurse Specialist CNS
https://www.readbyqxmd.com/read/26258832/waiting-for-the-antidote-the-journey-of-idarucizumab-as-a-potential-specific-reversal-agent-for-dabigatran-pradaxa
#17
Patricia Anne O'Malley
No abstract text is available yet for this article.
September 2015: Clinical Nurse Specialist CNS
https://www.readbyqxmd.com/read/26185953/dagibatran-etexilate-is-there-any-need-for-coagulation-monitoring-after-initiation
#18
Robert Hoepner, Volker Behrendt, Saskia Meves, Ralf Gold, Christos Krogias
INTRODUCTION: Activated prothrombin time (aPTT) and thrombin time (TT) can serve as indicators for anticoagulation effect of dabigatran etexilate (Pradaxa), the new oral reversible, competitive inhibitor of thrombin. Further, a significant elevation of these coagulation parameters might demonstrate an increased risk of bleeding probably due to an accumulation of dabigatran. CASE REPORTS: We present 2 cases of patients with atrial fibrillation as well as mild and moderate renal impairment, which were treated with dabigatran...
July 2015: Neurologist
https://www.readbyqxmd.com/read/26095540/direct-acting-oral-anticoagulants-pharmacology-indications-management-and-future-perspectives
#19
REVIEW
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
https://www.readbyqxmd.com/read/26047352/structure-guided-residence-time-optimization-of-a-dabigatran-reversal-agent
#20
Felix Schiele, Joanne van Ryn, Tobias Litzenburger, Michael Ritter, Daniel Seeliger, Herbert Nar
Novel oral anticoagulants are effective and safe alternatives to vitamin-K antagonists for anticoagulation therapy. However, anticoagulation therapy in general is associated with an elevated risk of bleeding. Idarucizumab is a reversal agent for the direct thrombin inhibitor, dabigatran etexilate (Pradaxa®) and is currently in Phase 3 studies. Here, we report data on the antibody fragment aDabi-Fab2, a putative backup molecule for idarucizumab. Although aDabi-Fab2 completely reversed effects of dabigatran in a rat model in vivo, we observed significantly reduced duration of action compared to idarucizumab...
2015: MAbs
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