Search results for "Thrombin"
showing 10 items of 201 documents
Predicting and Tuning Physicochemical Properties in Lead Optimization: Amine Basicities
2007
This review describes simple and useful concepts for predicting and tuning the pK(a) values of basic amine centers, a crucial step in the optimization of physical and ADME properties of many lead structures in drug-discovery research. The article starts with a case study of tricyclic thrombin inhibitors featuring a tertiary amine center with pK(a) values that can be tuned over a wide range, from the usual value of around 10 to below 2 by (remote) neighboring functionalities commonly encountered in medicinal chemistry. Next, the changes in pK(a) of acyclic and cyclic amines upon substitution by fluorine, oxygen, nitrogen, and sulfur functionalities, as well as carbonyl and carboxyl derivativ…
Increased thrombin generation and complement activation in patients with type IIA hyperlipoproteinemia: effects of simvastatin treatment
1997
Abstract The aim of this study was to demonstrate the existence of increased thrombin generation and complement activation in patients with type IIa primary hyperlipoproteinemia, but no signs of atherosclerotic vascular disease and to assess the effects of simvastatin treatment in these patients. We studied 40 patients with type IIa primary hyperlipoproteinemia and 40 healthy subjects matched for sex, age, body mass index, and smoking status. The study was divided into two phases. In the first phase, a cross-sectional comparison of lipid and hemostatic patterns was performed between patients and controls. In the second phase, we assessed the effect of a persistent reduction in cholesterol s…
Effect of gemfibrozil treatment on fibrinolysis system in patients with hypertriglyceridemia
1992
Abstract The effect of gemfibrozil on lipidic, coagulative, and fibrinolytic pattern was studied in 20 patients with primary type IV hyperlipoproteinemia. After a 4-week stabilization period during which administration of lipid-lowering drugs was stopped and an isocaloric diet (20% protein, 30% fat, and 50% carbohydrates) was prescribed, 20 patients (12 men and 8 women; mean age, 38 ± 4 years; body mass index, 23.4 ± 1.5) suffering from primary hypertriglyceridemia were included in this study and treated for a 12-week period with gemfibrozil (600 mg BID). Every 4 weeks the following parameters were checked: glycemia, triglycerides, total cholesterol, high density lipoprotein-cholesterol, to…
Evaluation of thrombin generation in classical Philadelphianegative myeloproliferative neoplasms / Evaluarea generării trombinei în neoplasmele mielo…
2016
Abstract Introduction: Patients with Philadelphia-negative chronic myeloproliferative neoplasms (Ph-MPN), polycytemia vera (PV), essential thrombocythaemia (ET) and primary myelofibrosis (PMF), are prone to develop thrombotic events. We aimed to investigate the coagulation status in their plasma using thrombin generation assay (TGA), a functional global assay, on Ceveron® Alpha. Materials and methods: The samples were collected from 89 consecutive Ph-negative MPN patients and from 78 controls into K2EDTA and CTAD tubes for blood cell counts, TGA and coagulation screening tests. Thrombin generation was analysed in platelet-poor plasma using Technothrombin® TGA assay kit. Results: We found a …
Exosomes from metastatic cancer cells transfer amoeboid phenotype to non-metastatic cells and increase endothelial permeability: their emerging role …
2017
AbstractThe goal of this study was to understand if exosomes derived from high-metastatic cells may influence the behavior of less aggressive cancer cells and the properties of the endothelium. We found that metastatic colon cancer cells are able to transfer their amoeboid phenotype to isogenic primary cancer cells through exosomes, and that this morphological transition is associated with the acquisition of a more aggressive behavior. Moreover, exosomes from the metastatic line (SW620Exos) exhibited higher ability to cause endothelial hyperpermeability than exosomes from the non metastatic line (SW480Exos). SWATH-based quantitative proteomic analysis highlighted that SW620Exos are signific…
Evidence for Impaired Hepatic Vitamin K1 Metabolism in Patients Treated with N-Methyl-Thiotetrazole Cephalosporins
1984
SummaryIn 8 patients on no oral intake and with parenteral alimentation, administration of cephalosporins with N-methyl-thiotetrazole side chain (moxalactam, cefamandole), was associated with prolongation of prothrombin time, appearance in the circulation of descarboxy-prothrombin (counter immunoelectrophoresis and echis carinatus assay) and diminution of protein C. Acute administration of 10 mg vitamin Ki was followed by the transient appearance of vitamin K1 2,3-epoxide, indicating an impaired hepatocellular regeneration of vitamin K1 from the epoxide. Impaired hepatic vitamin K1 metabolism, tentatively ascribed to the N-methyl-thiotetrazole group, is one (but possibly not the only) cause…
Manejo perioperatorio de los anticoagulantes orales directos en cirugía urgente y sangrado. Monitorización y tratamiento hemostático
2015
There is an almost unanimous consensus on the management of the direct new oral anticoagulants, dabigatran, rivaroxaban, and apixaban in elective surgery. However, this general consensus does not exist in relation with the direct new oral anticoagulants use in emergency surgery, especially in the bleeding patient. For this reason, a literature review was performed using the MEDLINE-PubMed. An analysis was made of the journal articles, reviews, systematic reviews, and practices guidelines published between 2000 and 2014 using the terms "monitoring" and "reversal". From this review, it was shown that the routine tests of blood coagulation, such as the prothrombin time and activated partial th…
Clinical characteristics of COVID-19 patients in Latvia under low incidence in Spring 2020
2020
ABSTRACTBackgroundCOVID-19 is a new infectious disease with severe disease course and high mortality in some groups. Blood tests on admission to the hospital can be useful for stratification of patients and timely correction. Our study investigated the clinical features of COVID-19 patients in Latvia and differences in blood tests in groups with different disease severity.MethodsThe retrospective study included 100 patients hospitalized in Riga East Clinical University Hospital in Spring 2020. The severity of the disease course was classified by the presence of pneumonia and its combination with respiratory failure. We have assessed blood cells’ count, hemoglobin, hematocrit, erythrocyte se…
The impact of whole blood processing and freezing conditions on the quality of therapeutic plasma prepared from whole blood
2014
Background The quality of whole blood (WB)-derived plasma preparations has been the subject of several studies, but there has been a lack of robust, comparative data for the different methods of processing and freezing. Study Design and Methods Six WB-derived plasma units were pooled and split (n = 16) and frozen within either 8 or 24 hours after WB collection, stored at 4°C or at room temperature (RT), and then frozen either slowly at −20°C or rapidly to below −30°C. Plasma units were tested for fibrinogen, Factor (F)V, FVII, FVIII, FXI, and von Willebrand factor (VWF), protein C (PC), protein S (PS) activity and free PS, prothrombin time, and partial thromboplastin time. Results FVIII was…
D-Dimer, Thrombin-Antithrombin III-Komplex (TAT) und Prothrombinfragment 1+2 (PTF)
1997
Two groups of 15 patients each with disseminated intravascular coagulation in association with septic disease were treated with low-molecular-weight heparin (lmw-heparin) in different dosages (group I: 1.5-5 IE/kg body weight (BW) per hour; group II: 8-15 IE/kg BW). We studied the levels of D-dimer, thrombin-antithrombin III complex (TAT), prothrombin fragments 1 and 2 (PTF), and global tests of coagulation like prothrombin time (PT), activated partial thromboplastin time (PTT), thrombin time (TT) and platelet count, plasminogen activation (PA) and fibrinogen concentration to estimate the success of heparin therapy in the two groups. TT and fibrinogen concentration were not suitable to foll…