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Pharmacoepidemiology and Drug Safety Oct 2014Influenza infection places pregnant women at greater risk of morbidity and hospitalization. The use of oseltamivir to treat influenza increased markedly in all... (Review)
Review
PURPOSE
Influenza infection places pregnant women at greater risk of morbidity and hospitalization. The use of oseltamivir to treat influenza increased markedly in all population groups during the A/H1N1pdm09 pandemic, including pregnant women. Given this increase in exposure, a reassessment of the safety of oseltamivir in pregnancy was conducted.
METHODS
The Roche Global Safety Database was searched for all exposures to oseltamivir during pregnancy in the 13 years up to 30 April 2012.
RESULTS
Of the 2926 maternal exposures to oseltamivir retrieved from the Safety Database, pregnancy outcomes were known for 2128 women. Most exposures (>90%) were reported during or after the pandemic. The incidence of adverse pregnancy outcomes in exposed women was: spontaneous abortions, 2.9% (61/2128); therapeutic abortions, 1.8% (39/2128); and pre-term deliveries, 4.2% (84 of 2000 live births), values which are lower than background rates in the general population (women with or without influenza). Fetal outcomes were known in 1875 of the 2926 exposures. For the 81 reported birth defect cases, 11 occurred during the sensitive period for the respective defects. A review of these and other case reports of birth defects did not suggest that they resulted from oseltamivir exposure.
CONCLUSIONS
The data reviewed in this article reinforce the findings of a previous review, suggesting that oseltamivir is unlikely to cause adverse pregnancy or fetal outcomes.
Topics: Antiviral Agents; Databases, Factual; Embryonic Development; Female; Fetal Development; Humans; Influenza, Human; Oseltamivir; Pregnancy; Pregnancy Complications, Infectious; Pregnancy Outcome; Product Surveillance, Postmarketing
PubMed: 24995623
DOI: 10.1002/pds.3673 -
Medicinal Chemistry (Shariqah (United... Jul 2010Oseltamivir (has known by its brand name 'Tamiflu') is a prodrug, requiring ester hydrolysis for conversion to the active form, Oseltamivir carboxylate. Oseltamivir was... (Review)
Review
Oseltamivir (has known by its brand name 'Tamiflu') is a prodrug, requiring ester hydrolysis for conversion to the active form, Oseltamivir carboxylate. Oseltamivir was the first orally active neuraminidase inhibitor commercially developed by US based Gilead Sciences and is currently marketed by F. Hoffmann-La Roche (Roche). Oseltamivir is an antiviral drug which works by blocking the function of the viral neuraminidase protein. US FDA approved Oseltamivir for prophylaxis of uncomplicated influenza A and B. Currently, Oseltamivir is the only first line defense drug available for the treatment of Swine Flu. Orally Oseltamivir is well tolerated and effective in treatment of influenza in adolescents and adults, including the elderly and patients with chronic cardiac and/or respiratory disease. Many of the pharmaceutical companies targeted Oseltamivir as a block buster molecule. In present review, we have tried to cover chemistry, mode of binding, total synthesis, current patent status, adverse effect and clinical status of Oseltamivir giving emphasis on medicinal chemistry aspect.
Topics: Antiviral Agents; Dose-Response Relationship, Drug; Humans; Influenza Vaccines; Influenza, Human; Oseltamivir
PubMed: 20843284
DOI: 10.2174/1573406411006040247 -
Biochimica Et Biophysica Acta.... Mar 2024Oseltamivir belongs to the neuraminidase inhibitors, developed against the influenza virus, and registered under the trademark Tamiflu. Despite its long-term...
Oseltamivir belongs to the neuraminidase inhibitors, developed against the influenza virus, and registered under the trademark Tamiflu. Despite its long-term acquaintance, there is limited information in the literature about its physicochemical and structural properties in a lipid-water system. We present an experimentally determined partition coefficient with structural information on the interaction of oseltamivir with the model membrane, its possible location, and its effect on the membrane thermodynamics. The hydrophobic part of the lipid bilayer is affected to a moderate extent, which was proved by slight changes in thermal and structural properties. Hereby, interaction of oseltamivir with the phospholipid bilayer induces concentration dependent decrease of lateral pressure in the bilayer acyl chain region. Oseltamivir charges the bilayer surface positively, which results in the zeta potential increase and changes in anisotropic properties studied by the polarised light microscopy. At the highest oseltamivir concentrations studied, the multilamellar structure is extensively disturbed, likely due to electrostatic repulsion between the adjacent bilayers.
Topics: Oseltamivir; Antiviral Agents; Lipid Bilayers; Phospholipids; Phosphates
PubMed: 38211646
DOI: 10.1016/j.bbamem.2024.184273 -
Expert Opinion on Drug Metabolism &... Oct 2007The burden of seasonal influenza in children is poorly recognized, in spite of the potential for severe and even life-threatening illness and common secondary... (Review)
Review
The burden of seasonal influenza in children is poorly recognized, in spite of the potential for severe and even life-threatening illness and common secondary complications. Children are a primary reservoir for the spread of influenza to both family members and the community, which imposes a sizeable social and economic strain. Although vaccination is the primary intervention against childhood influenza, the antiviral neuraminidase inhibitors, oseltamivir and zanamivir, provide treatment options. Oseltamivir is administered orally to children aged > 1 year and has been shown to cost-effectively reduce the influenza disease burden and duration of viral shedding. Additionally, oseltamivir postexposure prophylaxis provides protective efficacy for children and families. Oseltamivir has shown excellent tolerability and a low potential for viral resistance in pediatric studies. In the event of an influenza pandemic, oseltamivir is expected to be at the forefront of containment strategies. This article reviews the pharmacology, efficacy and tolerability of oseltamivir as treatment and prophylaxis in children.
Topics: Antiviral Agents; Child; Disease Outbreaks; Drug Resistance, Viral; Drug and Narcotic Control; Humans; Influenza, Human; Oseltamivir; Quality-Adjusted Life Years
PubMed: 17916060
DOI: 10.1517/17425255.3.5.755 -
Viruses Nov 2023Influenza can cause respiratory infections, leading to significant morbidity and mortality in humans. While current influenza vaccines offer varying levels of...
Influenza can cause respiratory infections, leading to significant morbidity and mortality in humans. While current influenza vaccines offer varying levels of protection, there remains a pressing need for effective antiviral drugs to supplement vaccine efforts. Currently, the FDA-approved antiviral drugs for influenza include oseltamivir, zanamivir, peramivir, and baloxavir marboxil. These antivirals primarily target the virus, making them vulnerable to drug resistance. In this study, we evaluated the efficacy of the neuraminidase inhibitor, oseltamivir, against probenecid, which targets the host cells and is less likely to engender resistance. Our results show that probenecid has superior antiviral efficacy compared to oseltamivir in both in vitro replication assays and in vivo mouse models of influenza infection.
Topics: Humans; Animals; Mice; Oseltamivir; Influenza, Human; Probenecid; Influenza Vaccines; Antiviral Agents; Enzyme Inhibitors; Virus Replication; Neuraminidase; Drug Resistance, Viral
PubMed: 38140606
DOI: 10.3390/v15122366 -
The Journal of Antimicrobial... Apr 2010Influenza is a transmissible viral pathogen that continues to cause substantial morbidity and mortality. Oseltamivir is an orally administered antiviral medication that... (Review)
Review
Influenza is a transmissible viral pathogen that continues to cause substantial morbidity and mortality. Oseltamivir is an orally administered antiviral medication that selectively inhibits the influenza neuraminidase enzymes that are essential for viral replication. Treatment of infected children > or =1 year and adults of all ages may decrease the severity and duration of the symptoms of infection, while prophylactic dosing can prevent their onset. Oseltamivir is ingested in the form of a prodrug (oseltamivir phosphate) that is rapidly converted by hepatic esterases into the active metabolite, oseltamivir carboxylate. Oseltamivir carboxylate has high bioavailability and penetrates sites of infection at concentrations that are sufficient to inhibit viral replication. The pharmacokinetics of oseltamivir and oseltamivir carboxylate are dose proportional after repeated doses of up to 500 mg twice daily. This predictable profile means that oseltamivir is suitable for use in diverse patient populations, which may include young children and elderly patients, various ethnic groups and those with renal or hepatic impairment. As the potential for drug interactions is low, oseltamivir is also suitable for use in patients with co-morbid conditions who are likely to be receiving concomitant medications.
Topics: Administration, Oral; Antiviral Agents; Biological Availability; Drug Interactions; Humans; Influenza, Human; Oseltamivir; Prodrugs
PubMed: 20215135
DOI: 10.1093/jac/dkq015 -
Prescrire International Oct 2007More and more reports are linking severe and sometimes fatal neuropsychiatric disorders to oseltamivir, especially in children and adolescents. These disorders include...
More and more reports are linking severe and sometimes fatal neuropsychiatric disorders to oseltamivir, especially in children and adolescents. These disorders include suicidal behaviour, hallucinations, seizures, delirium and extrapyramidal disorders.
Topics: Adolescent; Adult; Child; Child, Preschool; France; Humans; Influenza, Human; Japan; Mental Disorders; Nervous System Diseases; Oseltamivir; Suicide; United States
PubMed: 17926837
DOI: No ID Found -
The Senior Care Pharmacist Sep 2020Oseltamivir is an effective agent for both the treatment and prevention of influenza, and its use is increasing. The package insert indicates that delirium and...
Oseltamivir is an effective agent for both the treatment and prevention of influenza, and its use is increasing. The package insert indicates that delirium and delirium-like events have been reported with the use of oseltamivir during postmarketing surveillance. The reports of neuropsychiatric events associated with oseltamivir are mainly in younger patients. To our knowledge, this is the first reported case of oseltamivirassociated neuropsychiatric events occurring with oseltamivir prophylaxis in an older adult.
A 74-year-old male with a history of mild neurocognitive disorder was given oseltamivir prophylaxis in the setting of an influenza outbreak during his rehabilitation facility stay and developed newfound psychiatric symptoms after administration of oseltamivir for influenza prophylaxis because of institutional outbreak. The patient recovered completely after cessation of oseltamivir.
We hope that our case report highlights the importance of careful consideration when prescribing oseltamivir prophylaxis in older people with or without previous history of neurocognitive disorder.Topics: Aged; Disease Outbreaks; Humans; Influenza, Human; Male; Neurocognitive Disorders; Oseltamivir
PubMed: 32807263
DOI: 10.4140/TCP.n.2020.394 -
Pediatric Nursing 2014Influenza is a highly contagious virus that causes an average of 20,000 hospitalizations a year in children under five years of age. As of March 30, 2013, the 2012-2013... (Review)
Review
Influenza is a highly contagious virus that causes an average of 20,000 hospitalizations a year in children under five years of age. As of March 30, 2013, the 2012-2013 flu season had seen 111 pediatric deaths, with 21 deaths in the 0- to 23-month-old range. Rates of influenza-associated hospitalization are substantially higher among infants and young children than among older children, and those under six months old are at the highest risk. Research shows that influenza vaccine is not as effective in children two years of age relative to adults, and the vaccine is not approved in infants younger than six months. Thus, preventing influenza and proper treatment are important for keeping this high-risk group safe from complications. With infants being highest at risk for complications and the extrapolation of efficacy and safety from the older population, the U.S. Food and Drug Administration (FDA) recently approved the use of the antiviral oseltamivir phosphate (Tamiflu) for treatment of uncomplicated influenza in patients two weeks and older. This young population is susceptible to the benefits as well as the risks of the drug. Health care providers must be aware of dosing, adverse reactions, and monitoring parameters to better treat and educate their patients.
Topics: Antiviral Agents; Child, Preschool; Contraindications; Humans; Infant; Infant, Newborn; Influenza Vaccines; Influenza, Human; Oseltamivir; United States
PubMed: 24757915
DOI: No ID Found -
Virulence Dec 2021Invasive pulmonary aspergillosis (IPA) is a life-threatening fungal infection occurring mainly in immunocompromised patients. We recently identified IPA as an emerging...
Invasive pulmonary aspergillosis (IPA) is a life-threatening fungal infection occurring mainly in immunocompromised patients. We recently identified IPA as an emerging co-infection with high mortality in critically ill, but otherwise immunocompetent influenza patients. The neuraminidase inhibitor oseltamivir is the current standard-of-care treatment in hospitalized influenza patients; however, its efficacy in influenza-associated pulmonary aspergillosis (IAPA) is not known. Therefore, we have established an imaging-supported double-hit mouse model to investigate the therapeutic effect of oseltamivir on the development of IAPA. Immunocompetent mice received intranasal instillation influenza A or PBS followed by orotracheal inoculation with 4 days later. Oseltamivir treatment or placebo was started at day 0, day 2, or day 4. Daily monitoring included micro-computed tomography and bioluminescence imaging of pneumonia and fungal burden. Non-invasive biomarkers were complemented with imaging, molecular, immunological, and pathological analysis. Influenza virus-infected immunocompetent mice developed proven airway IPA upon co-infection with , whereas non-influenza-infected mice fully cleared , confirming influenza as a risk factor for developing IPA. Longitudinal micro-CT showed pulmonary lesions after influenza infection worsening after co-infection, congruent with bioluminescence imaging and histology confirming pneumonia. Early oseltamivir treatment prevented severe influenza pneumonia and mitigated the development of IPA and associated mortality. A time-dependent treatment effect was consistently observed with imaging, molecular, and pathological analyses. Hence, our findings underscore the importance of initiating oseltamivir as soon as possible, to suppress influenza infection and mitigate the risk of potentially lethal IAPA disease.
Topics: Animals; Aspergillosis; Aspergillus; Aspergillus fumigatus; Coinfection; Disease Models, Animal; Humans; Influenza, Human; Invasive Pulmonary Aspergillosis; Mice; Oseltamivir; Pulmonary Aspergillosis; X-Ray Microtomography
PubMed: 34546839
DOI: 10.1080/21505594.2021.1974327