Rapid degradation of oseltamivir phosphate in clinical samples by plasma esterases.

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.

• Authors: Niklas Lindegardh, Geraint R Davies, Tinh Hien Tran, Jeremy Farrar, Pratap Singhasivanon, Nicholas P J Day, Nicholas J White
• Journal: Antimicrobial agents and chemotherapy (Antimicrob Agents Chemother) Vol. 50 Issue 9 Pg. 3197-9 (Sep 2006) ISSN: 0066-4804 [Print] United States
• PMID: 16940130 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, Non-U.S. Gov't)

Chemical References

• Antiviral Agents
• Organophosphates
• Prodrugs
• Oseltamivir
• Esterases

Topics

• Adult
• Antiviral Agents (blood, pharmacokinetics)
• Esterases (blood, metabolism)
• Female
• Humans
• Male
• Organophosphates (blood, pharmacokinetics)
• Oseltamivir (blood, pharmacokinetics)
• Prodrugs (pharmacokinetics)