The role of competitive binding to human serum albumin on efavirenz-warfarin interaction: a nuclear magnetic resonance study

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Abstract

The potential for co-prescription of the anti-human immunodeficiency virus (anti-HIV) drug efavirenz (EFV) and the oral anticoagulant warfarin (WAR) is currently high as EFV is a drug of choice for HIV type 1 infection and because cardiovascular disease is increasing among HIV-infected individuals. However, clinical reports of EFV-WAR interaction, leading to WAR overdosing, call for elucidation of the mechanisms involved in this drug-drug interaction. Here we present the first report demonstrating competition of the two drugs for the same binding site of human serum albumin. Using ligand-based nuclear magnetic resonance experiments, this study proves that EFV has an effect on the concentration of free WAR. This previously unidentified EFV-WAR interaction represents a potential risk factor that should be taken into account when considering treatment options. (c) 2013 Elsevier B.V. and the International Society of Chemotherapy. All rights reserved.
Original languageEnglish
Pages (from-to)443-446
Number of pages4
JournalInternational Journal Of Antimicrobial Agents
Volume42
Issue number5
DOIs
Publication statusPublished - 2013

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