Efavirenz is a drug of choice for adults and children infected with the human immunodeficiency virus. Notably, up to 35% of patients on efavirenz suffer from mood changes. This work aimed to investigate efavirenz biotransformation into 8-hydroxy-efavirenz as an up-stream event of mood changes and to evaluate the suitability of 8-hydroxy-efavirenz biomonitoring for the minimization of these manifestations. A case-control study with two age-matched groups of HIV-infected male patients was performed in a group without adverse central nervous system complaints (28 patients) and a group presenting mood changes (14 patients). The plasma concentration of non-conjugated 8-hydroxy-efavirenz was higher in patients with mood changes (p=0.020). An association between efavirenz and 8-hydroxy-efavirenz-glucuronide was found (Spearman r=0.414, p<0.010), only within therapeutic efavirenz concentrations. This correlation was not observed in patients with toxic (>4mg/L) plasma concentrations of the parent drug. We conclude that metabolism to 8-hydroxy-efavirenz is associated with efavirenz-related mood changes, which suggests that the concentration of this metabolite is a suitable parameter for therapeutic drug monitoring aimed at controlling these manifestations. Moreover, our data suggest that 8-hydroxy-efavirenz is able to cross the blood-brain barrier and that the peripheral detoxification of 8-hydroxy-efavirenz by glucuronidation may be inhibited by toxic efavirenz concentrations.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.toxlet.2016.08.009 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Barriers to PrEP use and adherence among adolescent girls and young women in Eastern, Southern, and Western Africa: a scoping review.
BMC Womens Health
December 2024
Department of Public Health Institute of Tropical Medicine, Antwerp, Belgium.
Background: Adolescent girls and young women (AGYW) are disproportionately affected by HIV. Globally, in 2022, an estimated 4000 AGYW 15-24 were newly infected with HIV weekly, and nearly 78% of these infections occurred in sub-Saharan Africa. Oral Pre-Exposure Prophylaxis (PrEP) is a key HIV prevention option within an overall HIV combination prevention approach with an efficacy of over 90% when taken correctly.
View Article and Find Full Text PDFBackground: It is crucial to consider cultural, religious, and socio-behavioural factors that may influence the acceptability of Minimally Invasive Tissues Sampling (MITS). MITS is being used to understand the causes of child death and conducted in nine countries within Africa and South Asia with the highest child mortality. Progress has been made in the development of laboratory infrastructures and training for physicians to do MITS, but many communities are concerned about the religious acceptability of taking samples from deceased children.
View Article and Find Full Text PDFMethane emissions from the riverine sandy wetlands on the Mongolia Plateau.
Environ Monit Assess
December 2024
State Key Laboratory of Vegetation and Environmental Change, Institute of Botany, Chinese Academy of Sciences, Nanxincun 20, Xiangshan, Beijing, 100093, China.
Methane (CH) processes and fluxes have been widely investigated in low-latitude tropical wetlands and high-latitude boreal peatlands. In the mid-latitude Mongolia Plateau, however, CH processes and fluxes have been less studied, particularly in riverine wetlands. In this study, in situ experiments were conducted in the riverine sandy wetlands of the Mongolia Plateau to gain a better understanding of CH emissions and their influencing mechanisms.
View Article and Find Full Text PDF[High expression of AURKB promotes malignant phenotype of osteosarcoma cells by activating nuclear factor-κB signaling DHX9].
Nan Fang Yi Ke Da Xue Xue Bao
December 2024
Department of Orthopedics, Nanchang 330006, China.
Objectives: To investigate the regulatory mechanism of aurora kinase B (AURKB) for promoting malignant phenotype of osteosarcoma cells.
Methods: HA-Vector or HA-AURKB was transfected in 293T cells to identify the molecules interacting with AURKB using immunoprecipitation combined with liquid chromatography-tandem mass spectrometry followed by verification with co-immunoprecipitation and Western blotting. In cultured osteosarcoma cells with lentivirus-mediated RNA interference of AURKB or DHX9 or their overexpression, the changes in cell proliferation, migration, and invasion activities were observed with EDU and Transwell assays.
[ Injection inhibits peritoneal dialysis fluid-induced endothelial-mesenchymal transition in HMrSV5 cells by regulating the TGF-β/Smad signaling pathway].
Nan Fang Yi Ke Da Xue Xue Bao
December 2024
Department of Physiology and Pharmacology, School of Integrated Chinese and Western Medicine, Taihe Traditional Chinese Medicine Hospital Affiliated to Anhui University of Chinese Medicine, Taihe 236600, China.
Objectives: To investigate the inhibitory effect of Danshen Injection on endothelial-mesenchymal transition (EndMT) induced by peritoneal dialysis fluid in HMrSV5 cells and the role of the TGF‑β/Smad signaling pathway in mediating this effect.
Methods: HMrSV5 cells cultured in 40% peritoneal dialysis solution for 72 h to induce EndMT were treated with 0.05%, 0.
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!