title: Pharmacokinetic, Pharmacogenetic, and Other Factors Influencing CNS Penetration of Antiretrovirals.
abstract: 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.
authors: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria; Centre for Drug Discovery Development and Production, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria.
authors: Jacinta Nwamaka
authors: 0000-0002-0640-7165
authors: JN
authors: Nwogu
authors: School 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, USA; Pharmacy Practice (Medicine and Pediatrics), School of Pharmacy and Pharmaceutical Sciences, University at Buffalo, 285 Kapoor Hall, Buffalo, NY 14214, USA; Center for Integrated Global Biomedical Sciences, University at Buffalo, Buffalo, NY 14203, USA.
authors: Qing
authors: 0000-0003-0123-9913
authors: Q
authors: Ma
authors: Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria; Centre for Drug Discovery Development and Production, Faculty of Pharmacy, University of Ibadan, Ibadan, Nigeria.
authors: Chinedum Peace
authors: CP
authors: Babalola
authors: Department of Clinical Pharmacology, University College Hospital, Ibadan, Nigeria.
authors: Waheed Adeola
authors: 0000-0003-2211-5442
authors: WA
authors: Adedeji
authors: School 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, USA; Pharmacy Practice (Medicine and Pediatrics), School of Pharmacy and Pharmaceutical Sciences, University at Buffalo, 285 Kapoor Hall, Buffalo, NY 14214, USA; Center for Integrated Global Biomedical Sciences, University at Buffalo, Buffalo, NY 14203, USA.
authors: Gene D
authors: GD
authors: Morse
authors: Division of Infectious Diseases, Center for Global Health, Feinberg School of Medicine, Northwestern University, 645 N. Michigan Avenue, Suite 900, Chicago, IL, USA.
authors: Babafemi
authors: B
authors: Taiwo