Agents Used in Antiretroviral Therapy

  • Authors: Philip Grant, MD (More Info)
  • Editors in Chief: Daniel R. Kuritzkes, MD; Joseph J. Eron, Jr., MD
  • Last Reviewed: 10/1/18 (What's New)

Summary

  • Because they are metabolized by cytochrome P450 3A4 enzymes, PIs (except nelfinavir) can be pharmacologically boosted
    • Boosting (with ritonavir or cobicistat) results in higher trough concentrations and/or longer half-lives, lower pill burden, and improved efficacy, but increases the potential for significant drug–drug interactions
    • Virologic failure of boosted PIs in first-line therapy has been associated with little or no emergence of major PI mutations[Eron 2006; Molina 2008; Ortiz 2008; Walmsley 2008]
  • Atazanavir
      Darunavir
        Lopinavir/Ritonavir

        Action required