Clinical implications of CNS penetration of antiretroviral drugs

Heather E. Wynn, Richard C. Brundage, Courtney V. Fletcher

Research output: Contribution to journalReview article

77 Citations (Scopus)

Abstract

The CNS serves as an important sanctuary site for HIV replication. The presence of HIV in this compartment may contribute to neurological complications in individuals infected with HIV. Understanding the CNS penetration capabilities of available antiretroviral agents may help clinicians to design treatment regimens with neuroprotective effects. Although numerous clinical studies and anecdotal reports have examined CSF antiretroviral drug exposure as a marker of CNS penetration, understanding the clinical relevance of these findings is difficult. Challenges with study design and subject recruitment often limit the investigator's ability to collect comprehensive data. Upon review of available data, the antiretroviral agents zidovudine, stavudine, lamivudine, nevirapine, efavirenz and indinavir demonstrate consistent penetration into the CSF. Zidovudine-, stavudine-, lamivudine-, didanosine- and protease inhibitor-based regimens also appear to suppress CSF viraemia or improve HIV neurological disease. These agents may be appropriate candidates for neuroprotective antiretroviral treatment regimens. Despite these data, several unanswered questions about the CSF antiretroviral drug exposure-response relationship still remain. Prospective, controlled studies examining this relationship are needed before absolute clinical recommendations are founded.

Original languageEnglish (US)
Pages (from-to)595-609
Number of pages15
JournalCNS Drugs
Volume16
Issue number9
DOIs
StatePublished - Jan 1 2002

Fingerprint

HIV
Anti-Retroviral Agents
Zidovudine
efavirenz
Pharmaceutical Preparations
Indinavir
Stavudine
Didanosine
Lamivudine
Viremia
Neuroprotective Agents
Protease Inhibitors
Research Personnel
Prospective Studies
Clinical Studies
stavudine, lamivudine, nevirapine drug combination

ASJC Scopus subject areas

  • Clinical Neurology
  • Psychiatry and Mental health
  • Pharmacology (medical)

Cite this

Clinical implications of CNS penetration of antiretroviral drugs. / Wynn, Heather E.; Brundage, Richard C.; Fletcher, Courtney V.

In: CNS Drugs, Vol. 16, No. 9, 01.01.2002, p. 595-609.

Research output: Contribution to journalReview article

Wynn, Heather E. ; Brundage, Richard C. ; Fletcher, Courtney V. / Clinical implications of CNS penetration of antiretroviral drugs. In: CNS Drugs. 2002 ; Vol. 16, No. 9. pp. 595-609.
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