Pharmacokinetics of zidovudine phosphorylation in human immunodeficiency virus-positive thai patients and healthy volunteers

Antimicrob Agents Chemother. 2000 Jul;44(7):1986-9. doi: 10.1128/AAC.44.7.1986-1989.2000.

Abstract

We assessed the pharmacokinetics of zidovudine (ZDV) in plasma and intracellular ZDV phosphate anabolites in peripheral blood mononuclear cells in Thai human immunodeficiency virus (HIV) type 1-infected patients and healthy volunteers. The plasma ZDV area under the concentration-time curve from 0 to 6 h (AUC(0-6)) was similar in patients and healthy volunteers (32.77 and 22.77 micromol/liter. h, respectively; confidence interval, -3.37 to 19. 92). Although the concentration of ZDV triphosphate (ZDVTP) was similar in the two groups, the ZDV monophosphate (ZDVMP) AUC(0-6) was significantly greater in HIV patients (1.12 pmol/10(6) cells) than in healthy volunteers (0.15 pmol/10(6) cells). In agreement with previously published data obtained with Caucasians, the significant difference in intracellular phosphorylation in Thai volunteers and HIV patients is primarily due to ZDVMP. Comparing the data from this study with the data obtained with Caucasians suggests no marked ethnic differences in ZDV phosphorylation.

Publication types

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

MeSH terms

  • Adult
  • Anti-HIV Agents / metabolism
  • Anti-HIV Agents / pharmacokinetics*
  • Dideoxynucleotides
  • Female
  • HIV Infections / metabolism*
  • Humans
  • Male
  • Phosphorylation
  • Reverse Transcriptase Inhibitors / metabolism
  • Reverse Transcriptase Inhibitors / pharmacokinetics*
  • Thailand
  • Thymine Nucleotides / blood
  • Zidovudine / analogs & derivatives
  • Zidovudine / blood
  • Zidovudine / metabolism
  • Zidovudine / pharmacokinetics*

Substances

  • Anti-HIV Agents
  • Dideoxynucleotides
  • Reverse Transcriptase Inhibitors
  • Thymine Nucleotides
  • 3'-azido-3'-deoxythymidine 5'phosphate
  • Zidovudine