Drug-drug interaction analysis of pyronaridine/artesunate and ritonavir in healthy volunteers

Am J Trop Med Hyg. 2012 Mar;86(3):489-495. doi: 10.4269/ajtmh.2012.11-0558.

Abstract

A multiple dose, parallel group study was conducted to assess for a drug-drug interaction between the pyronaridine/artesunate (PA) combination antimalarial and ritonavir. Thirty-four healthy adults were randomized (1:1) to receive PA for 3 days or PA with ritonavir (100 mg twice daily for 17 days, PA administered on Days 8-10). Pharmacokinetic parameters for pyronaridine, artesunate, and its active metabolite dihydroartemisinin (DHA) were obtained after the last PA dose and for ritonavir on Days 1 and 10. Ritonavir coadministration did not markedly change pyronaridine pharmacokinetics but resulted in a 27% increase in artesunate area under the curve (AUC) and a 38% decrease in DHA AUC. Ritonavir exposure was increased 3.2-fold in the presence of PA. The only relevant safety observations were increases in liver enzymes, only reaching a clinically significant grade in the PA + ritonavir arm. It was concluded that coadministered ritonavir and PA interact to alter exposure to artesunate, DHA, and ritonavir itself.

Publication types

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

MeSH terms

  • Adolescent
  • Adult
  • Antimalarials / administration & dosage*
  • Antimalarials / pharmacokinetics
  • Area Under Curve
  • Artemisinins / administration & dosage*
  • Artemisinins / pharmacokinetics
  • Artesunate
  • Drug Interactions
  • Female
  • HIV Protease Inhibitors / administration & dosage*
  • HIV Protease Inhibitors / pharmacokinetics
  • Humans
  • Male
  • Middle Aged
  • Naphthyridines / administration & dosage*
  • Naphthyridines / pharmacokinetics
  • Ritonavir / administration & dosage*
  • Ritonavir / pharmacokinetics
  • Young Adult

Substances

  • Antimalarials
  • Artemisinins
  • HIV Protease Inhibitors
  • Naphthyridines
  • Artesunate
  • artenimol
  • Ritonavir
  • pyronaridine