Pharmacology of Antiretroviral Therapies

Scott L. Letendre, J. Allen McCutchan, Ronald J. Ellis, Brookie M. Best and Edmund V. Capparelli

in The Neurology of AIDS

Third edition

Published on behalf of Oxford University Press

Published in print December 2011 | ISBN: 9780195399349
Published online September 2012 | e-ISBN: 9780199965199 | DOI:
Pharmacology of Antiretroviral Therapies

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  • Disorders of the Nervous System
  • Infectious Diseases


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After more than a decade of widespread use, combination antiretroviral therapy has not reduced the prevalence of HIV-associated neurocognitive disorders (HAND). Low drug concentrations in the brain, due to poor drug penetration of the blood-brain barrier by many antiretroviral therapies (ART), may partially explain why HAND persists or develops in treated patients. In this chapter, we review the relevant pharmacology of ART and accumulating evidence that the use of antiretrovirals that reach therapeutic concentrations in the central nervous system (CNS) are the best options to prevent and treat HIV-induced brain injury. Topics covered include an overview of the problem, pharmacokinetics of ART in the CNS, determinants of CNS penetration by ART, means of estimating CNS penetration by ART, pharmacodynamics of ART in the CNS, and the development of a clinically useful metric for the CNS effectiveness of antiretroviral drugs.

Chapter.  12175 words.  Illustrated.

Subjects: Disorders of the Nervous System ; Infectious Diseases

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