HIV-1 Virologic Rebound Due to Coadministration of Divalent Cations and Bictegravir
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REVIEW
HIV-1 Virologic Rebound Due to Coadministration of Divalent Cations and Bictegravir Alex E. Rock . Patricia L. DeMarais . Pamala T. Vergara-Rodriguez . Blake E. Max
Received: April 23, 2020 Ó The Author(s) 2020
ABSTRACT A potential drug-drug interaction exists between divalent and trivalent cations (Ca2?, Fe3?, Mg2?, Al3?, Zn2?) and HIV-1 integrase strand transfer inhibitors (INSTIs). There are limited case reports describing the clinical significance of this potential interaction and none to our knowledge identifying zinc co-administration with INSTIs. In this report we present a patient taking bictegravir/emtricitabine/tenofovir alafenamide who became viremic after ingesting zinc and calcium supplements and later was able to obtain virologic re-suppression after discontinuing supplements. This case represents a potential significant drug interaction between a commonly prescribed antiretroviral drug class and readily available over-the-counter divalent cation products.
Alex E. Rock and Blake E. Max contributed equally to the work.
Digital Features To view digital features for this article go to https://doi.org/10.6084/m9.figshare.12357842. A. E. Rock (&) B. E. Max Department of Pharmacy Practice, University of Illinois at Chicago, Chicago, IL, USA e-mail: [email protected] P. L. DeMarais P. T. Vergara-Rodriguez B. E. Max Ruth M. Rothstein CORE Center and Stroger Hospital of Cook County Health, Chicago, IL, USA
Keywords: AIDS; Calcium; Divalent cations; Drug interaction; HIV; HIV integrase inhibitors; INSTI; Integrase strand transfer inhibitors; Zinc Key Summary Points Why carry out this study? Integrase inhibitors, the newest class of antiretrovirals, are considered a part of first-line HIV therapy and commonly utilized. They are well tolerated and interact with very few other medications. However, a class drug-drug absorption interaction between integrase inhibitors and divalent cations is a notable exception. We observed a case of HIV treatment failure secondary to high doses of concomitant zinc supplementation with Biktarvy. Zinc is often not mentioned as a divalent cation of concern in the literature or package inserts. What was learned from the study? It is possible to fail Biktarvy therapy if high enough doses of zinc are administered. Diligent medication reconciliation, HIV and antiretroviral stewardship are important when assessing HIV treatment failure.
Infect Dis Ther
INTRODUCTION Integrase inhibitors (INSTIs) have become the preferred backbone for HIV treatment-naı¨ve patients because they are well tolerated, highly effective and infrequently interact with other medications [1]. However, a potential drug-drug interaction exists between divalent and trivalent cations (Ca2?, Fe3?, Mg2?, Al3?, Zn2?) and INSTIs. HIV-1 integrase enzyme has a catalytic site that coordinates two divalent magnesium cations essential for viral DNA integration [2]. Therefore, administration of divalent cations in the form of calcium, iron or magnesium supplements with INSTIs could result in a decrease in I
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