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Apixaban - Metabolism, Pharmacologic Properties and Drug Interactions.
Curr Drug Metab
September 2018
Department of Hematology and Transfusiology, National Center of Hemostasis and Thrombosis, Comenius University in Bratislava, Jessenius Faculty of Medicine in Martin, Martin University Hospital, Martin, 2 Kollarova Street, Martin, 03659. Slovakia.
Background: Apixaban is an oral, potent, highly selective, reversible and direct inhibitor of activated coagulation factor X, that is the end point of the intrinsic and extrinsic coagulation pathway. Additionally, apixaban has the capacity to indirectly inhibit thrombin-induced platelet aggregation. This new oral anticoagulant represents an immediate-release form of peroral drug with quick dissolution, linear pharmacokinetics, good bioavailability and rapid onset and offset of action.
View Article and Find Full Text PDFThe data that episodes and sequels of venous thromboembolism (VTE) are recorded in a significant percentage of patients receiving standard anticoagulants as VTE prophylaxis (unfractionated, low-molecular-weight heparin and vitamin K inhibitors) as well as the fact that these drugs have significant limitations and that they may cause serious side-effects in some patients indicate the need for the introduction of new anticoagulant drugs. Fondaparinux, a selective inhibitor of Factor Xa, administered following major orthopedic surgeries having a high risk for the development of VTE, is more efficient than enoxaparin sodium used in European and North-American approved doses. The increased incidence of major bleeding (excluding fatal) due to fondaparinux could be perhaps lowered by dosage reduction in patients with a mildly decreased creatinine clearance.
View Article and Find Full Text PDFIntroduction: We conducted a prospective observational study in cardiac arrest survivors treated with mild induced hypothermia, evaluating different platelet function tests at hypo- and normothermia. We also investigated the relation between gastric emptying and vasodilator stimulated phosphoprotein (VASP).
Methods: Comatose survivors of out of hospital cardiac arrest were included and divided into two groups, depending on whether dual platelet inhibition with peroral ticagrelor and aspirin was given or not.
[Effect of a novel fibrinolytic enzyme FA-I on thrombosis and thrombolysis].
Sichuan Da Xue Xue Bao Yi Xue Ban
March 2009
College of Animal Science and Technology, Northwest A&F University, Yangling 712100, China.
Objective: To study the effect of FA-I, a novel fibrinolytic enzyme isolated from the metabolite of Arthrobacter sp. DR-536, on thrombosis and thrombolysis in vivo.
Methods: The anticoagulated blood model of mise were administered with FA-I orally.
Arginine mimetic structures in biologically active antagonists and inhibitors.
Curr Med Chem
January 2007
Faculty of Pharmacy, University of Ljubljana, Askerceva7, 1000 Ljubljana, Slovenia.
Peptidomimetics have found wide application as bioavailable, biostable, and potent mimetics of naturally occurring biologically active peptides. L-Arginine is a guanidino group-containing basic amino acid, which is positively charged at neutral pH and is involved in many important physiological and pathophysiological processes. Many enzymes display a preference for the arginine residue that is found in many natural substrates and in synthetic inhibitors of many trypsin-like serine proteases, e.
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