Lower atovaquone/proguanil concentrations in patients taking efavirenz, lopinavir/ritonavir or atazanavir/ritonavir

AIDS. 2010 May 15;24(8):1223-6. doi: 10.1097/QAD.0b013e3283389129.

Abstract

HIV-infected travellers frequently use atovaquone/proguanil as malaria prophylaxis. We compared atovaquone/proguanil pharmacokinetics between healthy volunteers and HIV-infected patients taking efavirenz, lopinavir/ritonavir or atazanavir/ritonavir. The geometric mean ratio (95% confidence interval) area under the curve (AUC)0-->t for atovaquone relative to the healthy volunteers was 0.25 (0.16-0.38), 0.26 (0.17-0.41) and 0.54 (0.35-0.83) for patients on efavirenz, lopinavir/ritonavir and atazanavir/ritonavir, respectively. Proguanil plasma concentrations were also significantly lower (38-43%). Physicians should be alert for atovaquone/proguanil prophylaxis failures in patients taking efavirenz, lopinavir/ritonavir or atazanavir/ritonavir.

Trial registration: ClinicalTrials.gov NCT00421473.

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Alkynes
  • Atazanavir Sulfate
  • Atovaquone / blood*
  • Benzoxazines / administration & dosage
  • Benzoxazines / pharmacokinetics
  • Cyclopropanes
  • Drug Administration Schedule
  • Female
  • HIV Infections / drug therapy*
  • HIV Protease Inhibitors
  • HIV-1*
  • Humans
  • Lopinavir
  • Male
  • Middle Aged
  • Oligopeptides / administration & dosage
  • Oligopeptides / pharmacokinetics
  • Proguanil / blood*
  • Pyridines / administration & dosage
  • Pyridines / pharmacokinetics
  • Pyrimidinones / administration & dosage
  • Pyrimidinones / pharmacokinetics
  • Ritonavir / administration & dosage
  • Ritonavir / pharmacokinetics
  • Young Adult

Substances

  • Alkynes
  • Benzoxazines
  • Cyclopropanes
  • HIV Protease Inhibitors
  • Oligopeptides
  • Pyridines
  • Pyrimidinones
  • Lopinavir
  • Atazanavir Sulfate
  • efavirenz
  • Ritonavir
  • Proguanil
  • Atovaquone

Associated data

  • ClinicalTrials.gov/NCT00421473