These characteristics underpin the use of oseltamivir in the diverse patient populations that are likely to be affected by seasonal and pandemic influenza viruses. Funding for this manuscript and the Supplement to which it belongs was provided by F. Funding for the medical writing support was provided by F. This article is part of a Supplement sponsored by F. Hoffmann-La Roche Ltd. National Center for Biotechnology Information , U.
J Antimicrob Chemother. Brian E. Author information Copyright and License information Disclaimer. Hoffmann-La Roche Inc. This article has been cited by other articles in PMC. Abstract Influenza is a transmissible viral pathogen that continues to cause substantial morbidity and mortality. Keywords: mechanism of action, dosing, drug interactions. Introduction Influenza is an infectious viral agent that continues to cause considerable morbidity and mortality.
Open in a separate window. Figure 1. Figure 2. Table 1 Inhibitory concentrations IC 50 s of oseltamivir carboxylate against different neuraminidase subtypes in vitro 5 , 7 — 9. Pharmacokinetics of oseltamivir and OC To effectively limit viral replication and the viral load, therapeutic concentrations of OC must be achieved at all sites of infection and maintained for the duration of the dosing interval.
Figure 3. Influence of patient demographics and ethnicity Overall, there are no clinically relevant differences in the pharmacokinetics of oseltamivir or OC between healthy volunteers and infected patients; this applies in adults of different sexes, ages and weights. Figure 4. Influence of age Exposure to oseltamivir in elderly patients increases in proportion to the usual age-related decline in renal function.
Figure 5. Drug interactions Patients with influenza often take over-the-counter medications to ease their symptoms. Funding Funding for this manuscript and the Supplement to which it belongs was provided by F. Transparency declarations This article is part of a Supplement sponsored by F. The author is employed by F.
References 1. Nicholson KG. Human influenza. Textbook of Influenza. Oxford, UK: Blackwell Science; Moscona A. Neuraminidase inhibitors for influenza. N Engl J Med. Tamiflu SmPC. Tamiflu Summary of Product Characteristics. Clinical pharmacokinetics of the prodrug oseltamivir and its active metabolite Ro Clin Pharmacokinet. Oseltamivir carboxylate is effective against all subtypes of influenza neuraminidase.
Pandemic H1N1 - Update Antiviral Res. Comparison of the anti-influenza virus activity of RWJ with those of oseltamivir and zanamivir. Antimicrob Agents Chemother. Oral administration of a prodrug of the influenza virus neuraminidase inhibitor GS protects mice and ferrets against influenza infection.
Safety and pharmacology of oseltamivir in clinical use. In addition, two sets of guidelines were included. Severity of illness was significantly reduced by oseltamivir in previously healthy adults, and the frequency and duration of fever was significantly reduced in previously healthy adults and children. Oseltamivir reduces the duration of cough, fever, time to resolution of illness and frequency of hospitalization in both previously healthy adults, children and gat riskh adults.
The frequencies of secondary complications like bronchitis, sinusitis, otitis media, pneumonia, in addition to antibiotic use, were also reduced in most patients. Nausea was reported more often in previously healthy adults given oseltamivir than placebo 4. Emesis was reported by The adverse events were transient and of mild to moderate character. Headache was reported with a higher frequency in the oseltamivir group than in the placebo group in adults gat riskh 8.
Conclusions: Oseltamivir is a well tolerated orally active neuraminidase inhibitor which significantly reduces the duration of symptomatic illness and hastens the return to normal levels of activity when initiated promptly in patients with naturally acquired influenza.
It therefore represents a useful therapeutic alternative to zanamivir especially in patients who prefer oral administration or who have an underlying respiratory disorder and the M2 inhibitors amantadine and rimantadine because of its broader spectrum of anti-influenza activity and lower likelihood of resistance in patients with influenza.
In addition, although annual vaccination remains the best means of influenza prevention, there may be a place for oseltamivir in providing household prophylaxis or adjunctive prophylaxis in high-risk vaccinated patients during an outbreak of the disease or for use in patients in whom vaccination is unsuitable or ineffective.
Abstract Oseltamivir is a prodrug of oseltamivir carboxylate Ro , GS , a potent and selective inhibitor of the neuraminidase glycoprotein essential for replication of influenza A and B viruses.
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