Clinical implications of antiretroviral pharmacokinetics and pharmacodynamics in the CNS

The prevalence of HIV-associated brain disease remains high in the combination antiretroviral era. Factors associated with the development of HIV-associated neurocognitive impairment remain poorly understood. The selection of an antiretroviral regimen that can successfully penetrate the CNS compartment and control cerebrospinal fluid HIV replication may prove a crucial strategy in preventing the emergence and progression of HIV-associated neurocognitive impairment. Different antiretroviral agents and drug classes vary in their ability to penetrate the CNS. In this review, data on the CNS penetration of antiretrovirals are evaluated, including the clinical studies examining their relevance. Prospective studies examining the effect of different treatment strategies on CNS clinical outcomes are needed.