Exploiting pharmacokinetics to optimise antiretroviral therapy

Stephen L Becker MD; Richard MW Hoetelmans PharmD PhD.

Updated in April 2002 by Stephen L Becker MD

The application of pharmacologic principles to HIV therapeutics has advanced significantly during the past two years.

Pharmacology sessions at the major HIV peer review meetings are now routine, as researchers have applied basic observations of pharmacokinetics, pharmacodynamics and, recently, pharmacogenomics to antiretroviral therapies. Drug-drug interactions are now explicitly exploited to improve drug exposure, correlations of viral susceptibility and drug exposures have been used to conceptualise the needed drug levels to inhibit viral replication, and greater understanding of the intracellular compartment of effect and drug transporters are examples of recent work in the field. This report will summarise the fundamental pharmacologic concepts applied to HIV therapeutics and review the clinical application of pharmacokinetically enhanced antiretroviral regimens.

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