2016
DOI: 10.1128/aac.00280-16
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Abstract: Efavirenz (EFZ) has been associated with neuropsychiatric side effects. Recently, the 8-hydroxy-EFZ (8OH-EFZ) metabolite has been shown to be a potent neurotoxin in vitro, inducing neuronal damage at concentrations of 3.3 ng/ml. EFZ induced similar neuronal damage at concentrations of 31.6 ng/ml. We investigated the effect of genotype and blood-brain barrier integrity on EFZ metabolite concentrations in cerebrospinal fluid (CSF). We measured CSF drug concentrations in subjects from two separate study populatio… Show more

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Cited by 18 publications
(16 citation statements)
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“…In this regard, it is worth mentioning that in vitro BBB membrane also present a concentration difference of FD between upper and lower chamber of the BBB model that might influence the faster release of FD to the media at the lower chamber. In addition, previous studies have also established the unformulated EFV exposure can disrupt the integrity of BBB and possible toxicity to BBB endothelial cells 40 , 41 . This might also allow more drug to pass through the BBB in a shorter period of time.…”
Section: Discussionmentioning
confidence: 97%
See 1 more Smart Citation
“…In this regard, it is worth mentioning that in vitro BBB membrane also present a concentration difference of FD between upper and lower chamber of the BBB model that might influence the faster release of FD to the media at the lower chamber. In addition, previous studies have also established the unformulated EFV exposure can disrupt the integrity of BBB and possible toxicity to BBB endothelial cells 40 , 41 . This might also allow more drug to pass through the BBB in a shorter period of time.…”
Section: Discussionmentioning
confidence: 97%
“…EFV is one of the very effective NNRTIs that has been in use in present combined antiretroviral therapy (cART) for the treatment of HIV-1 infection. However, its low bioavailability, poor pharmacokinetics, and subsequent drug resistance have made it necessary to optimize therapeutic delivery agents to make EFV more targeted and effective 39 41 . Among the many nanocarbon materials that have been investigated for use as drug carriers, ND, is the most promising due to its many favorable properties, including, chemical inertness, biocompatibility, and easy availability compared to other nanocarbon materials 17 .…”
Section: Discussionmentioning
confidence: 99%
“…It is an important and widely used drug in HIV(human immunodeficiency virus) therapy [1,2]. Efavirenz is used as part of a first-line treatment and is very effective in suppressing plasma viral load [2,3]. However, there are concerns over central nervous system (CNS) toxicity related to the drug's use [1,3].…”
Section: Introductionmentioning
confidence: 99%
“…The mechanisms responsible for the CNS toxicity of this drug are yet to be resolved. Efavirenz is metabolised by Cytochrome P450 enzymes and has a number of metabolites [2,[4][5][6]. There are two main metabolites of efavirenz, that is 7-and 8-hydroxefavirenz.…”
Section: Introductionmentioning
confidence: 99%
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