Cerebrospinal fluid abacavir concentrations in HIV‐positive patients following once‐daily administration

Abstract

Abacavir is a widely used nucleotide reverse transcriptase inhibitor, for which cerebrospinal fluid (CSF) exposure has been previously assessed in twice-daily recipients. We studied abacavir CSF concentrations in 61 and nine HIV-positive patients taking abacavir once daily and twice daily, respectively. Patients on once-daily abacavir had higher plasma and CSF concentrations (96 vs. 22 ng ml , P = 0.038 and 123 vs. 49 ng ml , P = 0.038) but similar CSF-to-plasma ratios (0.8 vs. 0.5, P = 0.500). CSF abacavir concentrations were adequate in patients receiving once-daily treatment.

Contemporary Antiretroviral Therapy Dysregulates Iron Transport and Augments Mitochondrial Dysfunction in HIV-Infected Human Microglia and Neural-Lineage Cells

“…Tenofovir was not initially thought to achieve appreciable concentrations in human CSF, but significant TFV levels have been documented in brain tissue after oral dosing (median 148 ng/mL) [81,82]. Concentrations of most of the ARVs tested in hµglia experiments were based on published CSF drug levels reported in PWH who were receiving oral cART [61,[83][84][85]. Published data on CSF BIC levels were not available when these experiments were performed, but more recently, median total CSF BIC levels of 10.9 to 11.8 ng/mL have been reported (range 0.5 to 44.9) [86,87].…”