Pharmacokinetic evidence for the induction of lopinavir metabolism by efavirenz

Br J Clin Pharmacol. 2005 Jul;60(1):32-4. doi: 10.1111/j.1365-2125.2005.02369.x.

Abstract

Aims: The influence of efavirenz on lopinavir pharmacokinetics was investigated using a population approach.

Methods: Forty-five HIV patients treated with lopinavir/ritonavir plus efavirenz (A) and 24 patients treated with lopinavir/ritonavir plus nucleoside/nucleotide reverse transcriptase inhibitors (B) were studied.

Results: A relationship (P < 0.01) was established between the elimination rate constant of lopinavir (k(10)) and treatment with efavirenz. Mean k(10) was higher in group A than in group B (0.3838 vs 0.2810 h(-1)) (P < 0.001, 95% confidence interval for difference between means 0.1004, 0.1052).

Conclusions: These results suggest that lopinavir metabolism is induced by efavirenz.

Publication types

  • Clinical Trial
  • Controlled Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Alkynes
  • Anti-HIV Agents / metabolism*
  • Benzoxazines
  • Cyclopropanes
  • Drug Combinations
  • Drug Interactions
  • Female
  • HIV Protease Inhibitors / pharmacokinetics*
  • Humans
  • Lopinavir
  • Male
  • Oxazines / pharmacology*
  • Pyrimidinones / pharmacokinetics*
  • Ritonavir / pharmacokinetics*

Substances

  • Alkynes
  • Anti-HIV Agents
  • Benzoxazines
  • Cyclopropanes
  • Drug Combinations
  • HIV Protease Inhibitors
  • Oxazines
  • Pyrimidinones
  • Lopinavir
  • efavirenz
  • Ritonavir