Rapid degradation of oseltamivir phosphate in clinical samples by plasma esterases

Antimicrob Agents Chemother. 2006 Sep;50(9):3197-9. doi: 10.1128/AAC.00500-06.

Abstract

The anti-influenza drug oseltamivir is an ester prodrug activated by hepatic carboxylesterases. Plasma esterases also convert up to 31.8% of the parent compound to the active metabolite after 4 h ex vivo, with wide interindividual variation. This source of error is removed by adding the esterase inhibitor dichlorvos to blood collection tubes.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Antiviral Agents / blood
  • Antiviral Agents / pharmacokinetics*
  • Esterases / blood*
  • Esterases / metabolism
  • Female
  • Humans
  • Male
  • Organophosphates / blood
  • Organophosphates / pharmacokinetics
  • Oseltamivir / blood
  • Oseltamivir / pharmacokinetics*
  • Prodrugs / pharmacokinetics*

Substances

  • Antiviral Agents
  • Organophosphates
  • Prodrugs
  • Oseltamivir
  • Esterases