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Eur J Pharmacol. 2017 Oct 5;812:163-173. doi: 10.1016/j.ejphar.2017.07.016. Epub 2017 Jul 8.

Efavirenz: What is known about the cellular mechanisms responsible for its adverse effects.

Author information

1
Departamento de Farmacología, Facultad de Medicina, Universidad de Valencia, Valencia-Centro de Investigación Biomédica en Red-Enfermedades Hepáticas y Digestivas (CIBERehd), Valencia, Spain. Electronic address: nadezda.apostolova@uv.es.
2
Departamento de Farmacología, Facultad de Medicina, Universidad de Valencia, Valencia-Centro de Investigación Biomédica en Red-Enfermedades Hepáticas y Digestivas (CIBERehd), Valencia, Spain.
3
Unidad de Enfermedades Infecciosas - Medicina Interna, Hospital Clínico Universitario de Valencia, Spain.
4
Departamento de Farmacología, Facultad de Medicina, Universidad de Valencia, Valencia-Centro de Investigación Biomédica en Red-Enfermedades Hepáticas y Digestivas (CIBERehd), Valencia, Spain; FISABIO-Hospital Universitario Dr. Peset, Valencia, Spain.

Abstract

The HIV infection remains an important health problem worldwide. However, due to the efficacy of combined antiretroviral therapy (cART), it has ceased to be a mortal condition, becoming a chronic disease instead. Efavirenz, the most prescribed non-nucleoside analogue reverse transcriptase inhibitor (NNRTI), has been a key component of cART since its commercialization in 1998. Though still a drug of choice in many countries, its primacy has been challenged by the arrival of newer antiretroviral agents with better toxicity profiles and treatment adherence. The major side effects related to EFV have been widely described in clinical studies, however the mechanisms that participate in their pathogenesis remain largely ununderstood. This review provides an insight into the cellular and molecular mechanisms responsible for the development of the most significant undesired effects induced by efavirenz, both short- and long-term, revealed by in vitro and in vivo experimental pharmacological research. Growing evidence implicates the drug in energy metabolism, mitochondrial function, and other cellular processes involved in stress responses including oxidative stress, inflammation and autophagy.

KEYWORDS:

Adverse effects; Antiretroviral therapy; Efavirenz; HIV; Mechanisms; Toxicity

PMID:
28690189
DOI:
10.1016/j.ejphar.2017.07.016
[Indexed for MEDLINE]

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