tetano
Editor, Senior Moderator
Antimicrob Agents Chemother. 2012 Jun 25. [Epub ahead of print]
Safety, Tolerability and Pharmacokinetics of Intravenous Oseltamivir: Single- and Multiple-Dose Phase I Studies in Healthy Volunteers.
Brennan BJ, Davies B, Cirrincione-Dall G, Morcos PN, Beryozkina A, Chappey C, Bald? PA, Lennon-Chrimes S, Rayner CR.
Source
Hoffman-La Roche, Inc., Nutley, NJ, USA.
Abstract
Background There is an unmet need for an intravenous (IV) neuraminidase inhibitor, particularly for patients with severe influenza who cannot take oral medication.Methods Two phase I pharmacokinetic and safety studies of IV oseltamivir were carried out in healthy volunteers. The first was an open-label, randomized, four-period, two-sequence, single-dose trial of 100 mg, 200 mg and 400 mg oseltamivir IV over 2 h, and a 75 mg oral dose of oseltamivir. The second was a double-blind, placebo-controlled, parallel-group, multiple-dose study in which participants were randomized to 100 mg or 200 mg oseltamivir or placebo (normal saline) IV over 2 h, 12-hourly for 5 days.Result Exposure to the active metabolite oseltamivir carboxylate (OC) after dosing with 100 mg IV oseltamivir over 2 h was comparable with 75 mg administered orally. Single IV doses of oseltamivir up to 400 mg were well tolerated with no new safety signals. Multiple-dose data confirmed good tolerability of 100 mg and 200 mg oseltamivir, and showed efficacious OC exposures with 100 mg IV over 2 h twice daily for 5 days.Conclusions These results support further exploration of IV oseltamivir as an influenza treatment option for patients unable to take oral medication.
PMID:
22733065
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/22733065
Safety, Tolerability and Pharmacokinetics of Intravenous Oseltamivir: Single- and Multiple-Dose Phase I Studies in Healthy Volunteers.
Brennan BJ, Davies B, Cirrincione-Dall G, Morcos PN, Beryozkina A, Chappey C, Bald? PA, Lennon-Chrimes S, Rayner CR.
Source
Hoffman-La Roche, Inc., Nutley, NJ, USA.
Abstract
Background There is an unmet need for an intravenous (IV) neuraminidase inhibitor, particularly for patients with severe influenza who cannot take oral medication.Methods Two phase I pharmacokinetic and safety studies of IV oseltamivir were carried out in healthy volunteers. The first was an open-label, randomized, four-period, two-sequence, single-dose trial of 100 mg, 200 mg and 400 mg oseltamivir IV over 2 h, and a 75 mg oral dose of oseltamivir. The second was a double-blind, placebo-controlled, parallel-group, multiple-dose study in which participants were randomized to 100 mg or 200 mg oseltamivir or placebo (normal saline) IV over 2 h, 12-hourly for 5 days.Result Exposure to the active metabolite oseltamivir carboxylate (OC) after dosing with 100 mg IV oseltamivir over 2 h was comparable with 75 mg administered orally. Single IV doses of oseltamivir up to 400 mg were well tolerated with no new safety signals. Multiple-dose data confirmed good tolerability of 100 mg and 200 mg oseltamivir, and showed efficacious OC exposures with 100 mg IV over 2 h twice daily for 5 days.Conclusions These results support further exploration of IV oseltamivir as an influenza treatment option for patients unable to take oral medication.
PMID:
22733065
[PubMed - as supplied by publisher]
http://www.ncbi.nlm.nih.gov/pubmed/22733065