Pharmacokinetic, Pharmacogenetic, and Other Factors Influencing CNS Penetration of Antiretrovirals

Neurological complications associated with the human immunodeficiency virus (HIV) are a matter of great concern. While antiretroviral (ARV) drugs are the cornerstone of HIV treatment and typically produce neurological benefit, some ARV drugs have limited CNS penetration while others have been associ...

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Main Authors: Jacinta Nwamaka Nwogu, Qing Ma, Chinedum Peace Babalola, Waheed Adeola Adedeji, Gene D. Morse, Babafemi Taiwo
Format: Article
Language:English
Published: Wiley 2016-01-01
Series:AIDS Research and Treatment
Online Access:http://dx.doi.org/10.1155/2016/2587094
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author Jacinta Nwamaka Nwogu
Qing Ma
Chinedum Peace Babalola
Waheed Adeola Adedeji
Gene D. Morse
Babafemi Taiwo
author_facet Jacinta Nwamaka Nwogu
Qing Ma
Chinedum Peace Babalola
Waheed Adeola Adedeji
Gene D. Morse
Babafemi Taiwo
author_sort Jacinta Nwamaka Nwogu
collection DOAJ
description Neurological complications associated with the human immunodeficiency virus (HIV) are a matter of great concern. While antiretroviral (ARV) drugs are the cornerstone of HIV treatment and typically produce neurological benefit, some ARV drugs have limited CNS penetration while others have been associated with neurotoxicity. CNS penetration is a function of several factors including sieving role of blood-brain and blood-CSF barriers and activity of innate drug transporters. Other factors are related to pharmacokinetics and pharmacogenetics of the specific ARV agent or mediated by drug interactions, local inflammation, and blood flow. In this review, we provide an overview of the various factors influencing CNS penetration of ARV drugs with an emphasis on those commonly used in sub-Saharan Africa. We also summarize some key associations between ARV drug penetration, CNS efficacy, and neurotoxicity.
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series AIDS Research and Treatment
spelling doaj-art-24f12ceee2f64df0a3ee8322c41a7a7a2025-02-03T01:23:07ZengWileyAIDS Research and Treatment2090-12402090-12592016-01-01201610.1155/2016/25870942587094Pharmacokinetic, Pharmacogenetic, and Other Factors Influencing CNS Penetration of AntiretroviralsJacinta Nwamaka Nwogu0Qing Ma1Chinedum Peace Babalola2Waheed Adeola Adedeji3Gene D. Morse4Babafemi Taiwo5Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ibadan, Ibadan, NigeriaSchool of Pharmacy and Pharmaceutical Sciences and New York State Center of Excellence in Bioinformatics and Life Sciences, University at Buffalo, 701 Ellicott Street, Buffalo, NY 14203, USADepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ibadan, Ibadan, NigeriaDepartment of Clinical Pharmacology, University College Hospital, Ibadan, NigeriaSchool of Pharmacy and Pharmaceutical Sciences and New York State Center of Excellence in Bioinformatics and Life Sciences, University at Buffalo, 701 Ellicott Street, Buffalo, NY 14203, USADivision of Infectious Diseases, Center for Global Health, Feinberg School of Medicine, Northwestern University, 645 N. Michigan Avenue, Suite 900, Chicago, IL, USANeurological complications associated with the human immunodeficiency virus (HIV) are a matter of great concern. While antiretroviral (ARV) drugs are the cornerstone of HIV treatment and typically produce neurological benefit, some ARV drugs have limited CNS penetration while others have been associated with neurotoxicity. CNS penetration is a function of several factors including sieving role of blood-brain and blood-CSF barriers and activity of innate drug transporters. Other factors are related to pharmacokinetics and pharmacogenetics of the specific ARV agent or mediated by drug interactions, local inflammation, and blood flow. In this review, we provide an overview of the various factors influencing CNS penetration of ARV drugs with an emphasis on those commonly used in sub-Saharan Africa. We also summarize some key associations between ARV drug penetration, CNS efficacy, and neurotoxicity.http://dx.doi.org/10.1155/2016/2587094
spellingShingle Jacinta Nwamaka Nwogu
Qing Ma
Chinedum Peace Babalola
Waheed Adeola Adedeji
Gene D. Morse
Babafemi Taiwo
Pharmacokinetic, Pharmacogenetic, and Other Factors Influencing CNS Penetration of Antiretrovirals
AIDS Research and Treatment
title Pharmacokinetic, Pharmacogenetic, and Other Factors Influencing CNS Penetration of Antiretrovirals
title_full Pharmacokinetic, Pharmacogenetic, and Other Factors Influencing CNS Penetration of Antiretrovirals
title_fullStr Pharmacokinetic, Pharmacogenetic, and Other Factors Influencing CNS Penetration of Antiretrovirals
title_full_unstemmed Pharmacokinetic, Pharmacogenetic, and Other Factors Influencing CNS Penetration of Antiretrovirals
title_short Pharmacokinetic, Pharmacogenetic, and Other Factors Influencing CNS Penetration of Antiretrovirals
title_sort pharmacokinetic pharmacogenetic and other factors influencing cns penetration of antiretrovirals
url http://dx.doi.org/10.1155/2016/2587094
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