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Infect Dis Obstet Gynecol. 2008;2008:927574. doi: 10.1155/2008/927574.

The metabolism and transplacental transfer of oseltamivir in the ex vivo human model.

Author information

  • 1Department of Obstetrics and Gynecology, University of Texas Southwestern Medical Center Dallas, TX 75390-9032, USA. kevin.worley@mac.com

Abstract

Oseltamivir phosphate is extensively metabolized in the ex vivo human placenta model, and the transplacental passage of the metabolite oseltamivir carboxylate is incomplete.

OBJECTIVE:

To evaluate the metabolism and transplacental transfer of oseltamivir (Tamiflu) in the ex vivo human placental model.

STUDY DESIGN:

Perfusion studies were performed in six placentas from term, uncomplicated deliveries. Concentrations of oseltamivir phosphate (OP) that were 5-6 fold, 20-30 fold, and 600-800 fold above the therapeutic peak were tested, as neither OP nor its active metabolite, oseltamivir carboxylate (OC), could be detected at near-therapeutic concentrations. The transplacental transfer and accumulation of OC were assessed using the (14)C antipyrine reference method.

RESULTS:

OP was extensively metabolized to OC. In the 4 placentas with the highest concentration of OP, OC had a mean clearance index of 0.13 +/- 0.08, suggesting that transplacental passage occurs at a relatively low rate. Measurable fetal accumulation occurred in the two placentas with the highest initial concentrations.

CONCLUSIONS:

Oseltamivir phosphate was extensively metabolized in the ex vivo model. Transplacental transfer of the metabolite was incomplete and accumulation was minimal.

PMID:
18551180
[PubMed - indexed for MEDLINE]
PMCID:
PMC2413047
Free PMC Article
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