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Untersuchungen zur Eiweißbindung von Arzneistoffen durch kontinuierliche Ultrafiltration, 5. Mitt. Einfluß der S-Oxidation auf die Proteinbindung von Methylthioderivaten des Warfarins
Authors:Klaus Rehse  Madeleine Rothe  Kurt Ehlert
Abstract:Protein Binding of Drugs Determined by Continuous Ultrafiltration, V: Effect of S-Oxidation on the Protein Binding of Methylthio Derivatives of Warfarin The binding of three methylthio derivatives of warfarin to human serum albumin has been determined by continuous ultrafiltration. 4′-(Methylthio)warfarin S-oxide (2) has a free fraction that is seven to nine times as large as that of warfarin itself in the therapeutically used plasma concentrations (2.5–12.5 μmol/l). As 2 is effective in the same dose as warfarin and shows better pharmacokinetics it might improve the safety of oral anticoagulants.
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