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Effects of Antithrombotic and Results of Drug Screening
Published in Josef Hladovec, Antithrombotic Drugs in Thrombosis Models, 2020
Some new drugs were at a relatively early phase tested in animal models. Thus pyri- dazinone derivative C 85-3143 was tested in stenotic and freeze-injured carotids in rats, as well as in stenotic jugular veins of rabbits,731 peptide derivative of factor X in the Wessler- type model of vein thrombosis in rabbits,732 molsidomine and its metabolite SIN-1 in the rat mesenteric microcirculation,733 as well as in silver nitrate-induced venous and arterial thrombosis in rabbits.734 Diferuloyl methan (curcumin), isolated from the indian plant curcuma longa, was effective in a mouse DIC induced by intravenous collagen and epinephrine.41 Born and Kovacs97 successfully tested N-acetyl neuraminic acid in the microcirculation of rats and hamsters injured by laser shots. Herrmann et al.735 observed a marked antithrombotic activity in hamster cheek pouch microthrombosis induced by the fluorescein-isothiocyanate method after the vasodilating agent naftidrofuryl (probably blocking 5-HT2 receptors). Using the Homstra method with the polyethylene loop in the carotid artery Lecker and Kumar736 tested a new pyridazinone derivative. Ott and Smith737 investigated a naphthyridine derivative in rats with a polyethylene tubing inserted into the carotid artery (Chan’s method). The glycosaminoglycan sulodexide was successfully tested in electrically induced carotid artery thrombosis in rats.738
Drug treatment of varicose veins, venous edema, and ulcers
Published in Peter Gloviczki, Michael C. Dalsing, Bo Eklöf, Fedor Lurie, Thomas W. Wakefield, Monika L. Gloviczki, Handbook of Venous and Lymphatic Disorders, 2017
Dermatan sulfate (DS) is a glycosaminoglycan which selectively catalyzes the inactivation of thrombin by heparin cofactor II without interacting with antithrombin III. DS does not interact with other coagulation factors and, unlike heparin, is able to inactivate thrombin bound to fibrin or to the surface of an injured vessel. Two DS-containing compounds—sulodexide and, particularly, mesoglycan—have been clinically studied in a number of trials and found to be effective in the treatment of venous and arterial leg diseases. Sulodexide is a highly purified glycosaminoglycan with pro-fibrinolytic properties.20 A total of 235 patients were randomized to receive sulodexide or placebo for 3 months. The authors reported improved healing in the active treatment group compared to placebo. No further detailed work on this compound has been published.
Managing chronic kidney disease in diabetes patients with the latest chemical therapies
Published in Expert Review of Clinical Pharmacology, 2019
Sulodexide is mixture of low-molecular-weight heparin and dermatan sulfate to inhibit TGF-β production. In a dose ranging study, subjects with diabetes and microalbuminuria received sulodexide 50 mg, 100 mg, 200 mg, or placebo therapy, and the urinary albumin excretion rate served as the primary outcome. The dose-dependent reduction in albumin excretion rate was observed in all sulodexide groups in comparison to placebo after 4 months [34]. Subsequently, a larger randomized trial was performed to investigate the efficacy of sulodexide 200 mg/day in comparison to placebo, but this trial was terminated due to failure to detect significant difference between treatment and control groups on the changes in urinary protein or serum creatinine [35]. Now, two trials (ClinicalTrials.gov identifier: NCT00130208, ClinicalTrials.gov identifier: NCT01000545) examining the renoprotective effects of sulodexide are currently underway [36,37].
Extended oral anticoagulation after incident venous thromboembolism – a paradigm shift?
Published in Expert Review of Cardiovascular Therapy, 2020
Ida Ehlers Albertsen, Gregory Piazza, Mette Søgaard, Peter Brønnum Nielsen, Torben Bjerregaard Larsen
Sulodexide, a mixture of low-molecular-weight heparin and dermatan sulfate, and acetylsalicylic acid have also been investigated for extended treatment. Both drugs have been compared with placebo. In the Sulodexide in Secondary Prevention of Recurrent Deep Vein Thrombosis (SURVET) Study [31], unprovoked VTE patients who had completed 3–12 months of initial anticoagulant treatment were randomly assigned to sulodexide 500 lipasemic units twice daily or placebo for 2 years. Sulodexide was effective at reducing recurrence risk (4.9% vs. 9.7%) (HR 0.49; 0.27–0.92). There were no episodes reported of major bleeding, and the HR for clinically relevant non-major bleeding was 0.97; 0.14–6.88.
Secretory activity of the coronary artery endothelial cells in conditions of the peritoneal dialysis
Published in Renal Failure, 2022
Monika Misian, Ewa Baum, Andrzej Bręborowicz
We present results from a study in which the effects of overnight peritoneal dialysate effluents from CAPD patients dialyzed with high GDP fluid Dianeal 1.5% and their sera on the functional properties of coronary arterial endothelial cells were studied. Additionally, we show how these effects can be modulated by the drug Sulodexide, which is a mixture of natural glycosaminoglycans. Sulodexide has an anti-inflammatory and antithrombotic effect in venous diseases [15]. However, there are no data describing its effect in coronary artery endothelial cells (CAEC).