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Die Pharmazie Jun 2020A retrospective analysis was conducted on the use of oseltamivir phosphate in outpatients and inpatients in our hospital from February 2016 to February 2019. The...
A retrospective analysis was conducted on the use of oseltamivir phosphate in outpatients and inpatients in our hospital from February 2016 to February 2019. The indications, purposes, dosage, combination, and adverse reactions were analysed focussing on the rationality and safety of oseltamivir. The relationship between adverse reactions and age, allergic history, underlying diseases, and combined drug use were analysed to find the risk factors associated therewith. A total of 1795 adult patients and 3199 children were treated with oseltamivir phosphate. In the adult group 1481 patients (82.5%) and in the child group, 2602 patients (81.3%) received oseltamivir for therapeutic ourposes. The main clinical diagnoses were upper respiratory tract infection, bronchitis, and pneumonia. Only 767 cases (15.2%) were confirmed as influenza virus infection by virological examination, the rest were suspected influenza cases and clinically diagnosed influenza cases. For preventive drug use, an adult group comprising 314 cases (17.5%) and a child group with 597 cases (18.7%) were identified. The dosage and course of treatment were more standardised, but there were too many types of combined drugs, and the indications of preventive use were insufficient in some cases. A total of 106 adverse drug reactions (2.12%) was recorded, mainly affecting the digestive system and neuropsychiatric systems. The rate of adverse drug reactions was related to age and the number of drug combinations. Attention should also be paid to age, combination of drugs, and allergy history.
Topics: Adolescent; Adult; Age Factors; Aged; Aged, 80 and over; Antiviral Agents; Dose-Response Relationship, Drug; Female; Humans; Influenza, Human; Male; Middle Aged; Oseltamivir; Respiratory Tract Infections; Retrospective Studies; Risk Factors; Young Adult
PubMed: 32539927
DOI: 10.1691/ph.2020.0352 -
Prescrire International Feb 2016
Topics: Antiviral Agents; Humans; Oseltamivir
PubMed: 27042722
DOI: No ID Found -
The Journal of Infectious Diseases Apr 2020A synergistic effect of combination therapy with favipiravir and oseltamivir has been reported in preclinical models of influenza. However, no data are available on the...
BACKGROUND
A synergistic effect of combination therapy with favipiravir and oseltamivir has been reported in preclinical models of influenza. However, no data are available on the clinical effectiveness of combination therapy in severe influenza.
METHODS
Data from 2 separate prospective studies of influenza adults were used to compare outcomes between combination and oseltamivir monotherapy. Outcomes included rate of clinical improvement (defined as a decrease of 2 categories on a 7-category ordinal scale) and viral RNA detectability over time. Subhazard ratios (sHRs) were estimated by the Fine and Gray model for competing risks.
RESULTS
In total, 40 patients were treated with combination therapy and 128 with oseltamivir alone. Clinical improvement on day 14 in the combination group was higher than in the monotherapy group (62.5% vs 42.2%; P = .0247). The adjusted sHR for combination therapy was 2.06 (95% confidence interval, 1.30-3.26). The proportion of undetectable viral RNA at day 10 was higher in the combination group than the oseltamivir group (67.5% vs 21.9%; P < .01). No significant differences were observed in mortality or other outcomes.
CONCLUSIONS
Favipiravir and oseltamivir combination therapy may accelerate clinical recovery compared to oseltamivir monotherapy in severe influenza, and this strategy should be formally evaluated in a randomized controlled trial.
Topics: Aged; Amides; Antiviral Agents; Critical Illness; Drug Therapy, Combination; Female; Humans; Influenza, Human; Male; Middle Aged; Oseltamivir; Pyrazines; Retrospective Studies
PubMed: 31822885
DOI: 10.1093/infdis/jiz656 -
JPMA. the Journal of the Pakistan... Oct 2022Swine flu is mainly caused by influenza virus strain H1N1. This strain of influenza has been found to cause seasonal flu. Animals are common source of influenza virus,...
Swine flu is mainly caused by influenza virus strain H1N1. This strain of influenza has been found to cause seasonal flu. Animals are common source of influenza virus, in particular, pigs. Transmissions from animals to humans are reported on several occasions worldwide. These cases are usually mild to moderate in nature and are usually not fatal. Here we describe the case of a healthy woman from Haripur, Pakistan, who presented in the Emergency Department of Quaid-e-Azam International Hospital, Islamabad and later developed a lethal course of H1N1influenza virus that resulted in her death, despite of aggressive management with Osaltemivir and Antibiotics in the Intensive care unit. Osaltemivir resistance has emerged in many countries including Pakistan. There is a strong need for increasing surveillance and the laboratories that can test for antiviral resistance, particularly in a third world country like Pakistan.
Topics: Humans; Female; Animals; Swine; Oseltamivir; Antiviral Agents; Influenza A Virus, H1N1 Subtype; Influenza, Human; Drug Resistance, Viral
PubMed: 36661010
DOI: 10.47391/JPMA.4498 -
Bioorganic & Medicinal Chemistry May 2017In search of novel anti-influenza agents with higher potency, a series of acylguanidine oseltamivir carboxylate analogues were synthesized and evaluated against...
In search of novel anti-influenza agents with higher potency, a series of acylguanidine oseltamivir carboxylate analogues were synthesized and evaluated against influenza viruses (H1N1 and H3N2) in vitro. The representative compounds with strong inhibitory activities (IC <40nM) against neuraminidase (NA) were further tested against the NA from oseltamivir-resistant strain (H259Y). Among them, compounds 9 and 17 were potent NA inhibitors that exhibited a 5 and 11-fold increase in activity comparing with oseltamivir carboxylate (2, OC) against the H259Y mutant, respectively. Furthermore, the effect against influenza virus H259Y mutant (H1N1) replication and cytotoxicity assays indicated that compounds 9 and 17 exhibited a 20 and 6-fold increase than the parent compound 2, and had no obvious cytotoxicity in vitro. Moreover, the molecular docking studies revealed that the docking modes of compounds 9 and 17 were different from that of oseltamivir, and the new hydrogen bonds and hydrophobic interaction were formed in this case. This work provided unique insights in the discovery of potent inhibitors against NAs from wild-type and oseltamivir-resistant strains.
Topics: Animals; Antiviral Agents; Binding Sites; Cell Survival; Dogs; Drug Design; Enzyme Inhibitors; Guanidines; Influenza A Virus, H1N1 Subtype; Influenza A Virus, H3N2 Subtype; Madin Darby Canine Kidney Cells; Molecular Docking Simulation; Mutation; Neuraminidase; Oseltamivir; Protein Structure, Tertiary; Structure-Activity Relationship; Virus Replication
PubMed: 28385598
DOI: 10.1016/j.bmc.2017.03.052 -
American Journal of Health-system... Jan 2015Published evidence regarding the use of the antiinfluenza agent oseltamivir outside of the standard dosing recommendations is reviewed. (Review)
Review
PURPOSE
Published evidence regarding the use of the antiinfluenza agent oseltamivir outside of the standard dosing recommendations is reviewed.
SUMMARY
Oseltamivir is a neuraminidase inhibitor indicated for the treatment of uncomplicated influenza in patients two weeks of age or older who have been symptomatic for no more than two days; the recommended dosage is 75 mg twice daily by mouth for five days. A literature search identified six studies evaluating the effects of administering oseltamivir 48 hours or more after the onset of influenza symptoms, administering the drug at double the standard dose, or continuing therapy for more than five days. Two randomized controlled trials found that double-dose oseltamivir therapy conferred no significant survival benefit. The results of one retrospective study of intensive care unit (ICU) patients infected with the influenza H1N1 strain suggested improved survival among those who received oseltamivir no later than five days after symptom onset.
CONCLUSION
Oseltamivir may increase survival when used within five days of symptom onset in influenza H1N1-infected patients who require ICU admission. There appears to be no benefit in starting treatment more than 48 hours after symptom onset in hospitalized general medicine patients or outpatients infected with either H1N1 or other influenza strains or in doubling the dose of oseltamivir in hospitalized patients or outpatients. There are scant data supporting the use of oseltamivir for longer than five days in any patient population, with the possible exception of critically ill H1N1-infected ICU patients, who may benefit from extended treatment in some cases.
Topics: Animals; Humans; Influenza A Virus, H1N1 Subtype; Influenza, Human; Off-Label Use; Oseltamivir; Randomized Controlled Trials as Topic; Treatment Outcome
PubMed: 25550133
DOI: 10.2146/ajhp140390 -
BMC Complementary Medicine and Therapies Jul 2023The morbidity of influenza in children increased rapidly in decade. Reduning injection (RDN), a small but fine Chinese herbal formula, has antipyretic, antiviral,... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
The morbidity of influenza in children increased rapidly in decade. Reduning injection (RDN), a small but fine Chinese herbal formula, has antipyretic, antiviral, anti-inflammatory effects. We intend to evaluate the efficacy and safety of RDN for the influenza in children versus Oseltamivir, explore the possible antiviral mechanism of RDN and provide evidence-based medical evidence for rational clinical drug usage.
METHOD
We design a randomized, double-blind, double-dummy, parallel control of positive drug, multi-centre clinical study. According to the formula of mean superiority test, a total of 240 patients with influenza in children will be randomized 1:1 into the experimental group and control group. The experimental group will take RDN and Oseltamivir phosphate granule simulants and the control group will take Oseltamivir phosphate granule and RDN simulants. Each group will be treated for 5 days. The primary outcome measure is temperature recovery time, and the secondary outcome measures include time when the fever begins to subside, time and degree of disease to alleviate, disappearance rate of individual symptoms and so on. We will measure before enrollment and each 24 h after treatment for comparison.
DISCUSSION
The study is launched to evaluate the efficacy and safety of RDN for the treatment of influenza in children and to provide an alternative option for influenza in children.
TRIAL REGISTRATION
This study is registered in ClinicalTrials.gov as NCT04183725, registered on 3 December, 2019.
Topics: Humans; Child; Influenza, Human; Oseltamivir; Antiviral Agents; Double-Blind Method; Phosphates
PubMed: 37474974
DOI: 10.1186/s12906-023-04037-1 -
Molecules (Basel, Switzerland) Jul 2022The use of vaccinations and antiviral medications have gained popularity in the therapeutic management of avian influenza H7N9 virus lately. Antiviral medicines are more...
The use of vaccinations and antiviral medications have gained popularity in the therapeutic management of avian influenza H7N9 virus lately. Antiviral medicines are more popular due to being readily available. The presence of the neuraminidase protein in the avian influenza H7N9 virus and its critical role in the cleavage of sialic acid have made it a target drug in the development of influenza virus drugs. Generally, the neuraminidase proteins have common conserved amino acid residues and any mutation that occurs around or within these conserved residues affects the susceptibility and replicability of the influenza H7N9 virus. Herein, we investigated the interatomic and intermolecular dynamic impacts of the experimentally reported E119V mutation on the oseltamivir resistance of the influenza H7N9 virus. We extensively employed molecular dynamic (MD) simulations and subsequent post-MD analyses to investigate the binding mechanisms of oseltamivir-neuraminidase wildtype and E119V mutant complexes. The results revealed that the oseltamivir-wildtype complex was more thermodynamically stable than the oseltamivir-E119V mutant complex. Oseltamivir exhibited a greater binding affinity for wildtype (-15.46 ± 0.23 kcal/mol) relative to the E119V mutant (-11.72 ± 0.21 kcal/mol). The decrease in binding affinity (-3.74 kcal/mol) was consistent with RMSD, RMSF, SASA, PCA, and hydrogen bonding profiles, confirming that the E119V mutation conferred lower conformational stability and weaker protein-ligand interactions. The findings of this oseltamivir-E119V mutation may further assist in the design of compounds to overcome E119V mutation in the treatment of influenza H7N9 virus patients.
Topics: Animals; Antiviral Agents; Drug Resistance, Viral; Humans; Influenza A Virus, H7N9 Subtype; Influenza in Birds; Influenza, Human; Mutation; Neuraminidase; Oseltamivir
PubMed: 35889251
DOI: 10.3390/molecules27144376 -
The Medical Letter on Drugs and... Nov 2023
Topics: Humans; Antiviral Agents; Influenza, Human; Enzyme Inhibitors; Neuraminidase; Oseltamivir; Zanamivir
PubMed: 37935021
DOI: 10.58347/tml.2023.1689e -
Journal of Medicinal Chemistry Sep 2022With our continuous endeavors in seeking neuraminidase (NA) inhibitors, we reported herein three series of novel oseltamivir amino derivatives with the goal of exploring...
Iterative Optimization and Structure-Activity Relationship Studies of Oseltamivir Amino Derivatives as Potent and Selective Neuraminidase Inhibitors Targeting 150-Cavity.
With our continuous endeavors in seeking neuraminidase (NA) inhibitors, we reported herein three series of novel oseltamivir amino derivatives with the goal of exploring the druggable chemical space inside the 150-cavity of influenza virus NAs. Among them, around half of the compounds in were demonstrated to be better inhibitors against both wild-type and oseltamivir-resistant group-1 NAs than oseltamivir carboxylate (OSC). Notably, compounds , , , and showed more potent or equipotent antiviral activity against H1N1, H5N1, and H5N8 viruses compared to OSC in cellular assays. Furthermore, compounds and exhibited high metabolic stability in human liver microsomes (HLMs) and low inhibitory effect on main cytochrome P450 (CYP) enzymes, as well as low acute/subacute toxicity and certain antiviral efficacy . Also, pharmacokinetic (PK) and molecular docking studies were performed. Overall, and possess great potential to serve as anti-influenza candidates and are worthy of further investigation.
Topics: Antiviral Agents; Drug Resistance, Viral; Enzyme Inhibitors; Guanidines; Humans; Influenza A Virus, H1N1 Subtype; Influenza A Virus, H5N1 Subtype; Molecular Docking Simulation; Neuraminidase; Oseltamivir; Structure-Activity Relationship
PubMed: 35939763
DOI: 10.1021/acs.jmedchem.1c01970