Abstract
Infection by human immunodeficiency virus-1 (HIV) once had a near-certainly fatal prognosis. Today, HIV infection can be controlled due to the advent and deployment of antiretroviral therapy (ART), allowing HIV-infected (HIV+) patients to survive longer. HIV+ patients frequently experience comorbidities that stem, at least in part, from side effects induced by the long-term use of ART. HIV+ patients commonly exhibit microvascular alterations and disruptions of the blood–brain barrier (BBB), which may be caused or exacerbated by ART-induced toxicity. The BBB, being the crucial anatomic and biochemical interface between peripheral circulation and the central nervous system, is particularly exposed to potentially toxic effects of antiretroviral drugs (ARVds). This chapter analyzes the adverse effects related to the therapeutic use of ARVds in the context of BBB dysfunction and ART-induced toxicity. Moreover, it provides possible future approaches to HIV therapy, which may mitigate the toxicities observed in ART-treated patients.