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Management of Antiretroviral Therapy with Boosted Protease Inhibitors—Darunavir/Ritonavir or Darunavir/Cobicistat

A major challenge in the management of antiretroviral therapy (ART) is to improve the patient’s adherence, reducing the burden caused by the high number of drugs that compose the treatment regimens for human immunodeficiency virus positive (HIV+) patients. Selection of the most appropriate treatment...

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Autores principales: Marin, Ruxandra-Cristina, Behl, Tapan, Negrut, Nicoleta, Bungau, Simona
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8003312/
https://www.ncbi.nlm.nih.gov/pubmed/33803812
http://dx.doi.org/10.3390/biomedicines9030313
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author Marin, Ruxandra-Cristina
Behl, Tapan
Negrut, Nicoleta
Bungau, Simona
author_facet Marin, Ruxandra-Cristina
Behl, Tapan
Negrut, Nicoleta
Bungau, Simona
author_sort Marin, Ruxandra-Cristina
collection PubMed
description A major challenge in the management of antiretroviral therapy (ART) is to improve the patient’s adherence, reducing the burden caused by the high number of drugs that compose the treatment regimens for human immunodeficiency virus positive (HIV+) patients. Selection of the most appropriate treatment regimen is responsible for therapeutic success and aims to reduce viremia, increase the immune system response capacity, and reduce the incidence rate and intensity of adverse reactions. In general, protease inhibitor (PI) is one of the pillars of regimens, and darunavir (DRV), in particular, is frequently recommended, along with low doses of enzyme inhibitors as cobicistat (COBI) or ritonavir (RTV), by the international guidelines. The potential of clinically significant drug interactions in patients taking COBI or RTV is high due to the potent inhibitory effect on cytochrome CYP 450, which attracts significant changes in the pharmacokinetics of PIs. Regardless of the patient or type of virus, the combined regimens of DRV/COBI or DRV/RTV are available to clinicians, proving their effectiveness, with a major impact on HIV mortality/morbidity. This study presents current information on the pharmacokinetics, pharmacology, drug interactions, and adverse reactions of DRV; it not only compares the bioavailability, pharmacokinetic parameters, immunological and virological responses, but also the efficacy, advantages, and therapeutic disadvantages of DRV/COBI or DRV/RTV combinations.
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spelling pubmed-80033122021-03-28 Management of Antiretroviral Therapy with Boosted Protease Inhibitors—Darunavir/Ritonavir or Darunavir/Cobicistat Marin, Ruxandra-Cristina Behl, Tapan Negrut, Nicoleta Bungau, Simona Biomedicines Review A major challenge in the management of antiretroviral therapy (ART) is to improve the patient’s adherence, reducing the burden caused by the high number of drugs that compose the treatment regimens for human immunodeficiency virus positive (HIV+) patients. Selection of the most appropriate treatment regimen is responsible for therapeutic success and aims to reduce viremia, increase the immune system response capacity, and reduce the incidence rate and intensity of adverse reactions. In general, protease inhibitor (PI) is one of the pillars of regimens, and darunavir (DRV), in particular, is frequently recommended, along with low doses of enzyme inhibitors as cobicistat (COBI) or ritonavir (RTV), by the international guidelines. The potential of clinically significant drug interactions in patients taking COBI or RTV is high due to the potent inhibitory effect on cytochrome CYP 450, which attracts significant changes in the pharmacokinetics of PIs. Regardless of the patient or type of virus, the combined regimens of DRV/COBI or DRV/RTV are available to clinicians, proving their effectiveness, with a major impact on HIV mortality/morbidity. This study presents current information on the pharmacokinetics, pharmacology, drug interactions, and adverse reactions of DRV; it not only compares the bioavailability, pharmacokinetic parameters, immunological and virological responses, but also the efficacy, advantages, and therapeutic disadvantages of DRV/COBI or DRV/RTV combinations. MDPI 2021-03-18 /pmc/articles/PMC8003312/ /pubmed/33803812 http://dx.doi.org/10.3390/biomedicines9030313 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ).
spellingShingle Review
Marin, Ruxandra-Cristina
Behl, Tapan
Negrut, Nicoleta
Bungau, Simona
Management of Antiretroviral Therapy with Boosted Protease Inhibitors—Darunavir/Ritonavir or Darunavir/Cobicistat
title Management of Antiretroviral Therapy with Boosted Protease Inhibitors—Darunavir/Ritonavir or Darunavir/Cobicistat
title_full Management of Antiretroviral Therapy with Boosted Protease Inhibitors—Darunavir/Ritonavir or Darunavir/Cobicistat
title_fullStr Management of Antiretroviral Therapy with Boosted Protease Inhibitors—Darunavir/Ritonavir or Darunavir/Cobicistat
title_full_unstemmed Management of Antiretroviral Therapy with Boosted Protease Inhibitors—Darunavir/Ritonavir or Darunavir/Cobicistat
title_short Management of Antiretroviral Therapy with Boosted Protease Inhibitors—Darunavir/Ritonavir or Darunavir/Cobicistat
title_sort management of antiretroviral therapy with boosted protease inhibitors—darunavir/ritonavir or darunavir/cobicistat
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8003312/
https://www.ncbi.nlm.nih.gov/pubmed/33803812
http://dx.doi.org/10.3390/biomedicines9030313
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