Effect of efavirenz, nevirapine, etravirine, and raltegravir administration on the pharmacokinetics of ritonavir-boosted darunavir in a population of HIV-infected patients

AIDS Res Hum Retroviruses. 2013 Jan;29(1):42-6. doi: 10.1089/AID.2012.0188. Epub 2012 Dec 16.

Abstract

Abstract The influence of efavirenz, etravirine, raltegravir, and nevirapine administration on the pharmacokinetics of ritonavir-boosted darunavir was investigated using population pharmacokinetics analysis. The population was composed of 142 patients infected with HIV: darunavir plus nucleoside/nucleotide reverse transcriptase inhibitors (NRTI), 54 patients (group A); darunavir plus efavirenz±NRTI, 4 patients (group B); darunavir plus etravirine±NRTI, 5 patients (group C); darunavir plus nevirapine±NRTI, 21 patients (group D); darunavir plus raltegravir±NRTI, 38 patients (group E); and darunavir plus raltegravir and etravirine±NRTI, 20 patients (group F). A significant increase in darunavir clearance in combination with nevirapine (+66%) and efavirenz (+235%) was observed. A significant decrease (p<0.05) in trough plasma concentration was observed in groups B and D compared with the other groups. Our study indicates that the combination of ritonavir-boosted darunavir and etravirine or raltegravir has no significant influence on the pharmacokinetics of darunavir in contrast to the combination of ritonavir-boosted darunavir and nevirapine or efavirenz, which involves an increase in darunavir clearance and a decrease in the plasma concentration of darunavir.

Publication types

  • Clinical Trial

MeSH terms

  • Adult
  • Alkynes
  • Anti-HIV Agents / administration & dosage
  • Anti-HIV Agents / therapeutic use*
  • Antiretroviral Therapy, Highly Active / methods
  • Benzoxazines / administration & dosage
  • Benzoxazines / therapeutic use*
  • Cyclopropanes
  • Darunavir
  • Drug Synergism
  • Female
  • HIV Infections / drug therapy*
  • HIV Protease Inhibitors / administration & dosage
  • HIV Protease Inhibitors / pharmacokinetics
  • HIV Protease Inhibitors / therapeutic use*
  • Humans
  • Male
  • Nevirapine / administration & dosage
  • Nevirapine / therapeutic use*
  • Nitriles
  • Pyridazines / administration & dosage
  • Pyridazines / therapeutic use*
  • Pyrimidines
  • Pyrrolidinones / administration & dosage
  • Pyrrolidinones / therapeutic use*
  • Raltegravir Potassium
  • Ritonavir / administration & dosage
  • Ritonavir / pharmacokinetics
  • Ritonavir / therapeutic use*
  • Sulfonamides / administration & dosage
  • Sulfonamides / blood
  • Sulfonamides / pharmacokinetics
  • Sulfonamides / therapeutic use*

Substances

  • Alkynes
  • Anti-HIV Agents
  • Benzoxazines
  • Cyclopropanes
  • HIV Protease Inhibitors
  • Nitriles
  • Pyridazines
  • Pyrimidines
  • Pyrrolidinones
  • Sulfonamides
  • etravirine
  • Raltegravir Potassium
  • Nevirapine
  • efavirenz
  • Ritonavir
  • Darunavir