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dc.contributor.authorApostolova, Nadezda
dc.contributor.authorFunes, Haryes A.
dc.contributor.authorBlas García, Ana
dc.contributor.authorGalindo, Maria J.
dc.contributor.authorÁlvarez, Ángeles
dc.contributor.authorEsplugues, Juan V.
dc.identifier.citationAPOSTOLOVA, Nadezda, et al. Efavirenz and the CNS: what we already know and questions that need to be answered. Journal of Antimicrobial Chemotherapy, 2015, vol. 70, no 10, p. 2693-2708.ca_CA
dc.description.abstractThe NNRTI efavirenz has long been one of the most frequently employed antiretroviral drugs in the multidrug regimens used to treat HIV infection, in accordance with its well-demonstrated antiretroviral efficacy and favourable pharmacokinetics. However, growing concern about its adverse effects has sometimes led to efavirenz being replaced by other drugs in the initial treatment selection or to switching of therapy to efavirenz-free regimens in experienced patients. Neurological and neuropsychiatric reactions are the manifestations most frequently experienced by efavirenz-treated patients and range from transitory effects, such as nightmares, dizziness, insomnia, nervousness and lack of concentration, to more severe symptoms including depression, suicidal ideation or even psychosis. In addition, efavirenz has recently been associated with mild/moderate neurocognitive impairment, which is of specific relevance given that half of the patients receiving ART eventually suffer some form of HIVassociated neurocognitive disorder. The mechanisms responsible for efavirenz-induced neurotoxicity are unclear, although growing evidence points to disturbances in brain mitochondrial function and bioenergetics. This review offers a comprehensive overview of the current evidence on the interaction that efavirenz displays with the CNS, including the penetration and concentration of the drug in the brain. We discuss the prevalence, types and specificities of its side effects and recently uncovered cellular mechanisms that may be involved in their development.ca_CA
dc.description.sponsorShipFunding: grants PI14/00312 and CIBER CB06/04/0071 (both from Instituto de Salud Carlos III, Ministerio de Economía y Competitividad), PROMETEOII/2014/035 and GV/2014/118 (both from Generalitat Valenciana), and P1.1B-2014/15 (Universitat Jaume I). A. B.-G. is a recipient of a Juan de la Cierva contract (JCI-2012-15124, Ministerio de Economía y Competitividad). H. A. F. is the recipient of Predoctoral Trainee Research Grant from Fundación Juan Esplugues.ca_CA
dc.publisherOxford University Pressca_CA
dc.relation.isPartOfJournal of Antimicrobial Chemotherapy, 2015, vol. 70, no 10ca_CA
dc.rights© The Author 2015. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For Permissions, please e-mail: journals.permissions@oup.comca_CA
dc.titleEfavirenz and the CNS: what we already know and questions that need to be answeredca_CA

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