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

Sofia A Pereira

doi:10.1016/j.ijantimicag.2013.06.023

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

Sofia A Pereira

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9 Citations (Scopus)

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 language	English
Pages (from-to)	443-446
Number of pages	4
Journal	International Journal Of Antimicrobial Agents
Volume	42
Issue number	5
DOIs	https://doi.org/10.1016/j.ijantimicag.2013.06.023
Publication status	Published - 2013

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

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.",

keywords = "Warfarin, AFFINITY, Drug-protein binding, SITES, ANTIRETROVIRAL THERAPY, DRUG-INTERACTIONS, Drug-drug interactions, Human serum albumin, HIV-INFECTED PATIENTS, NMR, Efavirenz",

author = "Pereira, {Sofia A}",

year = "2013",

doi = "10.1016/j.ijantimicag.2013.06.023",

language = "English",

volume = "42",

pages = "443--446",

journal = "International Journal Of Antimicrobial Agents",

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publisher = "Elsevier Science B.V., Inc",

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T1 - The role of competitive binding to human serum albumin on efavirenz-warfarin interaction: a nuclear magnetic resonance study

AU - Pereira, Sofia A

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AB - 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.

KW - Warfarin

KW - AFFINITY

KW - Drug-protein binding

KW - SITES

KW - ANTIRETROVIRAL THERAPY

KW - DRUG-INTERACTIONS

KW - Drug-drug interactions

KW - Human serum albumin

KW - HIV-INFECTED PATIENTS

KW - NMR

KW - Efavirenz

U2 - 10.1016/j.ijantimicag.2013.06.023

DO - 10.1016/j.ijantimicag.2013.06.023

M3 - Article

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VL - 42

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EP - 446

JO - International Journal Of Antimicrobial Agents

JF - International Journal Of Antimicrobial Agents

SN - 0924-8579

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