Influence of tenofovir, nevirapine and efavirenz on ritonavir-boosted atazanavir pharmacokinetics in HIV-infected patients

Eur J Clin Pharmacol. 2006 Jul;62(7):523-6. doi: 10.1007/s00228-006-0122-2. Epub 2006 Jun 9.

Abstract

Objective: The influence of nevirapine, efavirenz and tenofovir co-administration on ritonavir-boosted atazanavir pharmacokinetics was investigated in HIV (human immunodeficiency virus)-infected patients.

Methods: A population pharmacokinetic analysis was performed in the context of therapeutic drug monitoring (87 patients, 121 samples).

Results: A significant increase of atazanavir clearance (Cl/F) was found when either tenofovir (group B), efavirenz (group C), or nevirapine (group D) were co administered with atazanavir/ritonavir in comparison with patients treated with atazanavir/ritonavir and nucleoside reverse transcriptase inhibitors (group A): 6.24+/-0.36 l h(-1) (group A) versus 7.42+/-0.25 l h(-1) (group B) versus 9.60+/-0.27 l h(-1) (group C) versus 17.53+/-0.57 l h(-1) (group D) (P<0.001). However, the decrease of the mean trough plasma concentration of atazanavir was significant only in group D: 1.02+/-0.86 mg/l (group A) versus 0.21+/-013 mg/l (group D) (P<0.001).

Conclusion: The increase in atazanavir clearance when it is used in combination with nevirapine, efavirenz and/or tenofovir suggests that therapeutic drug monitoring of atazanavir should be performed in such circumstances.

MeSH terms

  • Adenine / analogs & derivatives
  • Adenine / pharmacology
  • Adenine / therapeutic use
  • Adult
  • Alkynes
  • Antiretroviral Therapy, Highly Active
  • Atazanavir Sulfate
  • Benzoxazines
  • Cyclopropanes
  • Drug Interactions
  • Female
  • HIV / drug effects*
  • HIV Infections / drug therapy*
  • HIV Infections / virology*
  • HIV Protease Inhibitors / blood
  • HIV Protease Inhibitors / pharmacokinetics*
  • Humans
  • Male
  • Nevirapine / pharmacology
  • Nevirapine / therapeutic use
  • Oligopeptides / blood
  • Oligopeptides / pharmacokinetics*
  • Oligopeptides / pharmacology*
  • Organophosphonates / pharmacology
  • Organophosphonates / therapeutic use
  • Oxazines / pharmacology
  • Oxazines / therapeutic use
  • Pyridines / blood
  • Pyridines / pharmacokinetics*
  • Pyridines / pharmacology*
  • Retrospective Studies
  • Reverse Transcriptase Inhibitors / therapeutic use*
  • Ritonavir / pharmacology
  • Ritonavir / therapeutic use
  • Tenofovir

Substances

  • Alkynes
  • Benzoxazines
  • Cyclopropanes
  • HIV Protease Inhibitors
  • Oligopeptides
  • Organophosphonates
  • Oxazines
  • Pyridines
  • Reverse Transcriptase Inhibitors
  • Atazanavir Sulfate
  • Nevirapine
  • Tenofovir
  • Adenine
  • efavirenz
  • Ritonavir