Encyclopedia of AIDS

Living Edition
| Editors: Thomas J. Hope, Douglas Richman, Mario Stevenson

Antiretroviral Drug Penetration into the CNS Compartment

Living reference work entry
DOI: https://doi.org/10.1007/978-1-4614-9610-6_437-1

Definition

The central nervous system is reached and infected a few hours after HIV infection. Viral replication occurs in perivascular macrophages, in microglia, and, although restricted, in astrocytes: neuronal damage is believed to be a consequence of neurotoxin production by the aforementioned cells of the immune system. Such cells are reached by antiretroviral drugs either directly (crossing blood–brain and blood–cerebrospinal fluid barriers) or through cerebral extracellular fluid (drained into cerebrospinal fluid); for several drugs, cerebrospinal fluid concentrations have been shown to reflect cerebral interstitial fluid concentrations. The penetration of several compounds into the central nervous system has been shown to be highly variable and to depend on drugs’ (molecular weight, lipophilicity, ionization, plasma protein binding, transport mechanisms) and patients’ characteristics (age, blood flow, blood–brain barrier permeability). Although the exact amount of drug...

Keywords

Lamivudine Zidovudine Tenofovir Efavirenz Nevirapine 
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Copyright information

© Springer Science+Business Media New York 2015

Authors and Affiliations

  1. 1.Unit of Infectious Diseases, Department of Medical SciencesUniversity of TorinoTorinoItaly