Adjuvant antithrombotic therapy in ST-elevation myocardial infarction: A narrative review
This article reviews the major pharmacologic features of, and clinical evidence on, adjuvant medical therapy in patients with ST-elevation myocardial infarction (STEMI) treated with primary percutaneous coronary intervention. These drugs include oral antiplatelets (aspirin and P2Y12 inhibitors such as clopidogrel, prasugrel and ticagrelor), intravenous antiplatelet agents (the P2Y12 inhibitor cangrelor, GP IIb/IIIa inhibitors such as abciximab, eptifibatide and tirofiban), and intravenous anticoagulant agents (unfractionated heparin, low molecular weight heparin and bivalirudin).ResumoNeste artigo foram analisadas as princ...
Source: Revista Portuguesa de Cardiologia - June 13, 2019 Category: Cardiology Source Type: research
Clinical Evaluation of the Tolerability, Pharmacokinetics, and Inhibition of Platelet Aggregation of Eptifibatide in Healthy Chinese Subjects
AbstractThe present study aimed to evaluate the pharmacokinetic properties and antiplatelet aggregation activity of eptifibatide in healthy Chinese subjects. Eptifibatide (180 μg/kg) was administrated by 2 bolus injections 10 minutes apart, followed by a 2.0 μg/kg/min infusion for 24 hours. The eptifibatide pharmacokinetic and antiplatelet aggregation activities were evaluated using nonlinear mixed‐effects modeling and noncompartmental analysis. Safety assessments inc luded adverse events, hematology, and biochemistry tests. Twelve Chinese healthy subjects were enrolled and completed the study. Steady‐state concentra...
Source: Clinical Pharmacology in Drug Development - June 12, 2019 Category: Drugs & Pharmacology Authors: Li Liu,
Yanhua Ding,
Zheng Jiao,
Min Wu,
Cuiyun Li,
Jingrui Liu,
Chengjiao Liu,
Yue Hu,
Qingmei Li,
Hong Zhang Tags: Original Manuscript Source Type: research
Lipopolysaccharide-Induced Hemolysis Is Abolished by Inhibition of Thrombin Generation but Not Inhibition of Platelet Aggregation
AbstractIn human sepsis, hemolysis is an independent predictor of mortality, but the mechanisms evoking hemolysis have not been fully elucidated. Therefore, we tested the hypotheses that (1) lipopolysaccharide (LPS)-induced hemolysis is dependent on thrombin generation or platelet aggregation and (2) red cell membranes are weakened by LPS. Anesthetized male Wistar rats were subjected to LPS or vehicle for 240 min. The effects of hemostasis inhibition on LPS-induced hemolysis were investigated by use of the thrombin inhibitor argatroban or the platelet function inhibitor eptifibatide. Free hemoglobin concentration, red ce...
Source: Inflammation - June 6, 2019 Category: Allergy & Immunology Source Type: research
Routine Glycoprotein IIb/IIIa Inhibitor Therapy in ST-Segment Elevation Myocardial Infarction: A Meta-Analysis
ConclusionsRoutine GPI administration in STEMI resulted in mortality reduction, driven by reductions in recurrent ischemic events – however predominantly in trials pre-prasugrel/ticagrelor. Trials in contemporary STEMI management are needed to confirm these findings. (Source: Canadian Journal of Cardiology)
Source: Canadian Journal of Cardiology - May 8, 2019 Category: Cardiology Source Type: research
JZTX-V Targets the Voltage Sensor in Kv4.2 to Inhibit Ito Potassium Channels in Cardiomyocytes
Conclusion
In conclusion, JZTX-V effectively inhibited the Ito current and extended theAPD. The molecular mechanism underlying the inhibitory action of JZTX-V on Ito may involve recognition of a conserved binding motif on the S3–S4 linker. Hydrophobic force plays an important role in interactions between the toxin and channel, and the extracellular conformational space of Kv4 modulates toxin affinity. Moreover, the phospholipid membrane may be involved in binding to toxin. These findings broadened our understanding of the effects of JZTX-V on cardiac electrophysiology and further clarified the molecular mechanisms ...
Source: Frontiers in Pharmacology - April 15, 2019 Category: Drugs & Pharmacology Source Type: research
Development and application of a high-throughput liquid chromatography–tandem mass spectrometric method for the simultaneous determination of thymosin α1 and its recombinant human form in plasma and urine
Publication date: 5 June 2019Source: Journal of Pharmaceutical and Biomedical Analysis, Volume 170Author(s): Tingting Wang, Lei Yin, Hao Wang, John Paul Fawcett, Jingkai GuAbstractThymosin α1 (Thymalfasin, Tα1) is a naturally occurring polypeptide widely used as an immune system enhancer for the treatment of HIV/AIDS, hepatitis B and C, and cancer. Recombinant human Tα1 (rh-Tα1) lacking N-terminal acetylation (NTA) displays similar biological activity to Tα1 and has completed phase III clinical trials in China. To compare the pharmacokinetics of rh-Tα1 and Tα1 and establish whether they undergo mutual transmutation ...
Source: Journal of Pharmaceutical and Biomedical Analysis - March 22, 2019 Category: Drugs & Pharmacology Source Type: research
Development and application of a high-throughput liquid chromatography-tandem mass spectrometric method for the simultaneous determination of thymosin α1 and its recombinant human form in plasma and urine
Publication date: Available online 15 March 2019Source: Journal of Pharmaceutical and Biomedical AnalysisAuthor(s): Tingting Wang, Lei Yin, Hao Wang, John Paul Fawcett, Jingkai GuAbstractThymosin α1 (Thymalfasin, Tα1) is a naturally occurring polypeptide widely used as an immune system enhancer for the treatment of HIV/AIDS, hepatitis B and C, and cancer. Recombinant human Tα1 (rh-Tα1) lacking N-terminal acetylation (NTA) displays similar biological activity to Tα1 and has completed phase III clinical trials in China. To compare the pharmacokinetics of rh-Tα1 and Tα1 and establish whether they undergo mutual transmu...
Source: Journal of Pharmaceutical and Biomedical Analysis - March 16, 2019 Category: Drugs & Pharmacology Source Type: research
Contemporary Use of Glycoprotein IIb/IIIa Inhibitors in Patients with Left Ventricular Assist Devices
The efficacy of glycoprotein IIB/IIIA inhibitor (IIB/IIA) use in patients who receive left ventricular assist devices (LVAD) has not been well studied. A prior single center study of eptifibatide use for pump thrombosis in almost exclusively HeartMate II (HMII) LVAD patients concluded that the risks of such use outweighed the benefits. We sought to analyze the outcomes of IIB/IIIA use in our more contemporary cohort of mixed axial and centrifugal flow LVAD patients. (Source: The Journal of Heart and Lung Transplantation)
Source: The Journal of Heart and Lung Transplantation - March 16, 2019 Category: Transplant Surgery Authors: S. Duclos, K. Matsuda, S. Jimenez, M. Wheeler, K. Sallam, W. Hiesinger, D. Banerjee Tags: 1069 Source Type: research
Primary Exchange of Heart Mate II Comes with Less Mortality/Treatment Failure within Six Months Than Eptifibatide Treatment
We compared those who got a VAD exchange primarily vs those who got eptifibatide treatment to establish which strategy was most beneficial in avoiding the primary endpoint of death or re-thrombosis (Source: The Journal of Heart and Lung Transplantation)
Source: The Journal of Heart and Lung Transplantation - March 16, 2019 Category: Transplant Surgery Authors: M. Dickinson, M. Leacche, N. Manandhar Shrestha, T. Boeve, S.V. Jovinge, S. Lee Tags: 1081 Source Type: research
Comparative study of platelet aggregation and secretion induced by Bothrops jararaca snake venom and thrombin.
Abstract
Victims of Bothrops jararaca snakebites manifest bleedings, blood incoagulability, platelet dysfunction, and thrombocytopenia, and the latter has been directly implicated in the genesis of hemorrhagic diathesis. We addressed herein the direct effects of B. jararaca venom (BjV) on ex vivo platelet aggregation and granule secretion in washed human and mouse platelets. BjV directly aggregated platelets, but the extent of platelet aggregation was lower in human than mouse platelets. On the other hand, BjV (24.4 μg/mL) and thrombin (0.1 U/mL) induced a similar extent of ATP and platelet factor 4 (PF4)...
Source: Toxicon - January 21, 2019 Category: Toxicology Authors: Rosa JG, de Albuquerque CZ, de Moura Mattaraia VG, Santoro ML Tags: Toxicon Source Type: research
Perioperative Bridging With Glycoprotein IIb/IIIa Inhibitors Versus Cangrelor: Balancing Efficacy and Safety.
CONCLUSIONS: Eptifibatide, tirofiban, and cangrelor are preferred over abciximab as a perioperative bridge. The choice of agent should be tailored to clinical characteristics of the patient and institutional acquisition costs.
PMID: 30646761 [PubMed - as supplied by publisher] (Source: The Annals of Pharmacotherapy)
Source: The Annals of Pharmacotherapy - January 16, 2019 Category: Drugs & Pharmacology Authors: Van Tuyl JS, Newsome AS, Hollis IB Tags: Ann Pharmacother Source Type: research
The Interaction of Cross-Linked Fibrin Fragment D-Dimer with {alpha}IIb{beta}3 Requires Receptor Activation, Occurs at Sites Other Than the {gamma}-404-411 Sequence, and Contributes to Clot Retraction
Conclusion: We conclude that cross-linked fibrin fragment D-dimer, like fibrinogen fragment 'D98', interacts with activated αIIbβ3 via sites other than the -404-411 peptide, and that this interaction contributes to clot retraction.DisclosuresColler: Rockefeller University: Patents & Royalties: RUC-4; Platelet Biogenesis: Consultancy; Centocor: Patents & Royalties: Abciximab; CeleCor: Consultancy, Equity Ownership; Accumetrics: Patents & Royalties: VerifyNow Assays; Scholar Rock: Consultancy, Equity Ownership. (Source: Blood)
Source: Blood - November 21, 2018 Category: Hematology Authors: Zafar, H., Li, J., Buitrago, C., Nesic, D., Coller, B. S. Tags: 301. Vascular Wall Biology, Endothelial Progenitor Cells, and Platelet Adhesion, Activation, and Biochemistry: Platelet Signaling and Interaction with the Microenvironment Source Type: research
Sushi Domain Containing 2 (SUSD2) inhibits platelet activation and binding to high-grade serous ovarian carcinoma cells.
Authors: Lager TW, Roetman JJ, Kunkel J, Thacker M, Sheets JN, Egland KA, Miles CM, Larson MK, Gubbels JAA
Abstract
Platelets play a central role in primary hemostasis affecting tumor survival and metastases. Tumors induce platelets to aggregate and bind to the cancer cells, resulting in protection from immune surveillance and often leading to thrombocytosis. In ovarian cancer (OvCa), one-third of patients present with thrombocytosis, a diagnosis that correlates with shorter survival. SUSD2 (SUShi Domain containing 2), a type I transmembrane protein, shown to inhibit metastatic processes in high-grade sero...
Source: Platelets - October 21, 2018 Category: Hematology Tags: Platelets Source Type: research
Comparison of In-Hospital Bleeding and Cardiovascular Events with High-Dose Bolus Tirofiban and Shortened Infusion to Short-Duration Eptifibatide as Adjunctive Therapy for Percutaneous Coronary Intervention
Potent platelet inhibition is one of the most important medical interventions to prevent ischemic complications during and after percutaneous coronary intervention (PCI). Practice has evolved with the introduction of potent oral P2Y12 inhibitors that provide quick, effective platelet inhibition, and the need for routine glycoprotein IIb/IIIa inhibitors (GPIs) has decreased. Additionally, a shorter duration of GPI infusion has been shown to be safe with adequate oral antiplatelet loading, but clinical outcome data are limited to eptifibatide. (Source: The American Journal of Cardiology)
Source: The American Journal of Cardiology - September 26, 2018 Category: Cardiology Authors: Gabrielle L. Anderson, Jennifer L. Osborn, Scott D. Nei, Malcolm R. Bell, Gregory W. Barsness, Kristin C. Mara, Narith N. Ou Source Type: research
