CNS Drugs

, Volume 27, Issue 1, pp 31–55

CSF Penetration by Antiretroviral Drugs


  • Christine Eisfeld
    • Department of NeurologyUniversity of Münster
  • Doris Reichelt
    • Department of Internal MedicineUniversity of Münster
  • Stefan Evers
    • Department of NeurologyUniversity of Münster
    • Department of NeurologyUniversity of Münster
Review Article

DOI: 10.1007/s40263-012-0018-x

Cite this article as:
Eisfeld, C., Reichelt, D., Evers, S. et al. CNS Drugs (2013) 27: 31. doi:10.1007/s40263-012-0018-x


Severe HIV-associated neurocognitive disorders (HAND), such as HIV-associated dementia, and opportunistic CNS infections are now rare complications of HIV infection due to comprehensive highly active antiretroviral therapy (HAART). By contrast, mild to moderate neurocognitive disorders remain prevalent, despite good viral control in peripheral compartments. HIV infection seems to provoke chronic CNS injury that may evade systemic HAART. Penetration of antiretroviral drugs across the blood–brain barrier might be crucial for the treatment of HAND. This review identifies and evaluates the available clinical evidence on CSF penetration properties of antiretroviral drugs, addressing methodological issues and discussing the clinical relevance of drug concentration assessment. Although a substantial number of studies examined CSF concentrations of antiretroviral drugs, there is a need for adequate, well designed trials to provide more valid drug distribution profiles. Neuropsychological benefits and neurotoxicity of potentially CNS-active drugs require further investigation before penetration characteristics will regularly influence therapeutic strategies and outcome.

Copyright information

© Springer International Publishing Switzerland 2012