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Pharmacokinetics and diffusion into sputum of oseltamivir and oseltamivir carboxylate in cystic fibrosis adults

tetano

Editor, Senior Moderator
Antimicrob Agents Chemother. 2011 Jun 13. [Epub ahead of print]
Pharmacokinetics and diffusion into sputum of oseltamivir and oseltamivir carboxylate in cystic fibrosis adults.
Jullien V, Hubert D, Launay O, Babany G, Lortholary O, Sermet I.
Source

Universit? Paris Descartes, Facult? de M?decine; Assistance Publique - H?pitaux de Paris (AP-HP).
Abstract

Oseltamivir is a prodrug of oseltamivir carboxylate (OC), a neuraminidase inhibitor used for treatment and prevention of influenza. The pharmacokinetics of these 2 compounds were investigated after a single 75 mg oseltamivir dose in 6 patients with cystic fibrosis (CF). Means (? standard deviations) of area under the curve from time zero to infinity (AUC) were 173 ? 58 μg.h/L for oseltamivir, and 2256 ? 394 μg.h/for OC. The concentrations of OC in sputum 4-6 h and 22-26 h after the intake ranged from 4.1 to 62.2 μg/L. The AUC of OC was approximately 30 % lower than and significantly different from published values in volunteers. Based on the present results, and because the anti-A/H1N1 influenza efficacy of OC is related to its AUC/50 % effective concentration (EC(50)) ratio, an increase in oseltamivir unitary dose could be considered for the treatment of influenza in CF patients. This should nevertheless be confirmed by a controlled pharmacokinetic study performed on a larger number of patients.

PMID:
21670188
[PubMed - as supplied by publisher]

http://www.ncbi.nlm.nih.gov/pubmed/21670188
 
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