Efavirenz and Metabolites in Cerebrospinal Fluid: Relationship with CYP2B6 c.516G→T Genotype and Perturbed Blood-Brain Barrier Due to Tuberculous Meningitis

• Published in: Antimicrobial agents and chemotherapy Vol. 60; no. 8; pp. 4511 - 4518
• Main Authors: Nightingale, Sam, Chau, Tran Thi Hong, Fisher, Martin, Nelson, Mark, Winston, Alan, Else, Laura, Carr, Daniel F., Taylor, Steven, Ustianowski, Andrew, Back, David, Pirmohamed, Munir, Solomon, Tom, Farrar, Jeremy, Törok, M. Estée, Khoo, Saye
• Format: Journal Article
• Language: English
• Published: United States American Society for Microbiology 01.08.2016
• Subjects: Alkynes; Benzoxazines; Benzoxazines - pharmacology; Benzoxazines - therapeutic use; Blood-Brain Barrier; Cyclopropanes; Genotype; Pharmacology; Reverse Transcriptase Inhibitors; Reverse Transcriptase Inhibitors - pharmacology; Reverse Transcriptase Inhibitors - therapeutic use; Tuberculosis, Meningeal; Tuberculosis, Meningeal - drug therapy
• ISSN: 0066-4804; 1098-6596
• DOI: 10.1128/AAC.00280-16

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. W...