MSOP1016: Science of Medicines - Antiviral Agents in Influenza Quiz
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What is the main focus of Lecture 15 on Antiviral agents - Influenza?

  • Investigating the prophylactic strategies against the flu virus
  • Discussing the structure and life cycle of the influenza virus (correct)
  • Analyzing the generation of antibiotics for influenza treatment
  • Exploring different classes of anti-viral therapeutic agents

    • In terms of antiviral agents acting against RNA viruses, where can detailed information about flu virus be found?

  • Chapter 20: Antiviral agents in the 2013 edition of a particular book (correct)
  • Influenza Lecture 15 handouts provided by Dr. Edwards
  • An introduction to medicinal chemistry by Graham Patrick
  • Chapter 38 of Foye’s Principles of Medicinal Chemistry

    • What is the function of neuraminidase inhibitors like zanamivir and oseltamivir?

  • Enhancing the antigenic variation in viruses
  • Preventing the spread of RNA viruses
  • Promoting the generation of antibiotic resistance
  • Inhibiting a specific enzyme to treat influenza (correct)

    • What is a key learning outcome related to influenza discussed in Lecture 15?

    <p>Demonstrating knowledge of anti-viral therapeutic agents based on neuraminidase inhibitors</p> Signup and view all the answers

    Which book provides information about Neuraminidase inhibitors specifically in Chapter 38?

    <p>Foye’s Principles of Medicinal Chemistry</p> Signup and view all the answers

    What is emphasized in relation to the prophylactic strategies against the flu virus?

    <p>The significance of understanding antigenic variation for vaccination</p> Signup and view all the answers

    What is the primary cause of mortality associated with influenza?

    <p>Infecting elderly individuals</p> Signup and view all the answers

    Which neuraminidase inhibitor is classified as a transition state inhibitor?

    <p>Peramivir</p> Signup and view all the answers

    What is the primary role of neuraminidase during the influenza virus life cycle?

    <p>Assisting in virion progeny release</p> Signup and view all the answers

    Which type of sialic acid receptors do human influenza hemagglutinin molecules bind to?

    <p>a-2-6 receptors</p> Signup and view all the answers

    What is the key function of hemagglutinin in the influenza virus?

    <p>Binding the virus to the target host cell</p> Signup and view all the answers

    Which classification distinguishes influenza viruses based on surface glycoproteins?

    <p>'H &amp; N' classification</p> Signup and view all the answers

    'Swine Flu' is caused by which type of influenza virus?

    <p>H1N1</p> Signup and view all the answers

    What was the rationale behind the approval of Rimantadine in 1993?

    <p>Decreased viral resistance by targeting two mechanisms simultaneously</p> Signup and view all the answers

    What is the main role of Neuraminidase (NA) in the infectious process?

    <p>Catalyze the release of new viral particles from infected cells</p> Signup and view all the answers

    How did efforts to develop analogues against mutants of amantadine fare?

    <p>Successful in overcoming viral resistance</p> Signup and view all the answers

    What is the primary reason for the slow progress in developing selective Neuraminidase inhibitors?

    <p>Lack of knowledge about the receptor structure</p> Signup and view all the answers

    What is the mechanism of action of Adamantanes like Amantadine and Rimantadine against influenza A virus at low concentrations?

    <p>Blocking a viral ion channel protein</p> Signup and view all the answers

    What led to the development and approval of Neuraminidase inhibitors?

    <p>Progress in crystal structure molecular modelling of Neuraminidase</p> Signup and view all the answers

    What is the impact of changing the stereochemistry at C-4 in TS inhibitors?

    <p>Increases binding interactions</p> Signup and view all the answers

    In TS inhibitors, what was the result of replacing the glycerol chain with 4-amino?

    <p>Increases activity</p> Signup and view all the answers

    What is the effect of introducing a hydroxyl group in TS inhibitors' drug design?

    <p>Reduces the electron density of the double bond</p> Signup and view all the answers

    Which type of side chain interaction led to the best activity increase from methyl to propyl ethers in Oseltamivir drug design?

    <p>Alkoxy side chain</p> Signup and view all the answers

    What was observed about the activity when changing from propyl to butyl ether in Oseltamivir drug design?

    <p>Activity decreased</p> Signup and view all the answers

    What was the outcome of replacing hydroxyl groups with 4-amino groups in TS inhibitors?

    <p>Enhanced binding interactions</p> Signup and view all the answers

    How does changing from methyl to n-nonyl affect the activity in Oseltamivir drug design?

    <p>Activity drops after n-nonyl</p> Signup and view all the answers

    What is the role of ether analogues in Oseltamivir drug design?

    <p>Generate activity enhancements</p> Signup and view all the answers

    Why is introducing an R or S chiral center beneficial in TS inhibitors' drug design?

    <p>Suggests two hydrophobic pockets</p> Signup and view all the answers

    What is one disadvantage of converting Oseltamivir to GS4071 by esterases in the gastrointestinal tract for oral administration?

    <p>Conversion may not always be complete</p> Signup and view all the answers

    What type of interaction does the glycerol side chain at C-6 primarily have in the active site?

    <p>Hydrogen bonding with glutamate residues</p> Signup and view all the answers

    What is the major advantage of the pseudo-boat conformation for Neu5Ac2en in terms of interactions and stability?

    <p>Increased hydrogen bonding</p> Signup and view all the answers

    Which functional group replacement in TS inhibitors led to the compound being selective and active in vivo?

    <p>Guanidinium group</p> Signup and view all the answers

    What is a characteristic of Zanamivir (Relenza) that makes it effective against influenza A & B?

    <p>Low bioavailability</p> Signup and view all the answers

    What led to the rejection of Neu5Ac2en as a therapeutic agent despite good binding confirmation?

    <p>Inhibitory effect on mammalian NA</p> Signup and view all the answers

    How was the transition state (TS) formed in the development of Zanamivir as a neuraminidase inhibitor?

    <p>By introducing unsaturation between C-2 &amp; C-3</p> Signup and view all the answers

    What factor contributed to the high selectivity of Zanamivir for influenza A NA?

    <p>Presence of a guanidinium group</p> Signup and view all the answers

    Which interaction type was crucial for the 1000-fold increase in activity seen in Zanamivir compared to Neu5Ac2en?

    <p>Van der Waals interactions</p> Signup and view all the answers

    'Why was Neu5Ac2en inactive in vivo despite its confirmed binding efficacy in crystal structures?' was a question asked due to its inhibitory effect on which type of NAs?

    <p>Mammalian NAs</p> Signup and view all the answers

    In the context of developing neuraminidase inhibitors, what characteristic made Zanamivir differ from Neu5Ac2en and led to its FDA approval?

    <p>Higher polarity and better bioavailability</p> Signup and view all the answers

    Which strain of influenza virus was primarily responsible for the 2009 swine flu pandemic?

    <p>A/H1N1</p> Signup and view all the answers

    What type of vaccine is preferred for children aged 2-17 years, unless contraindicated?

    <p>Live influenza vaccine</p> Signup and view all the answers

    Which strain of virus does the nasal spray flu vaccine and some injected vaccines also offer protection against in 2017/18?

    <p>B/Phuket/3073/2013-like virus</p> Signup and view all the answers

    Which strain of flu particularly affects children in 2017/18?

    <p>Influenza B</p> Signup and view all the answers

    Which type of flu vaccine is not recommended for pregnant women?

    <p>Live influenza vaccine</p> Signup and view all the answers

    Which strain of virus was identified as a risk factor for the elderly and people with long-term health conditions in 2017/18?

    <p>A/H3N2</p> Signup and view all the answers

    Which strain of virus was identified as the cause of a recent outbreak in a commercial poultry flock near Swindon?

    <p>H5N6 subtype of avian influenza</p> Signup and view all the answers

    Which strain of virus was identified as the cause of a recent outbreak in a commercial duck flock in County Tyrone?

    <p>H5N6 subtype of avian influenza</p> Signup and view all the answers

    Which strain of virus is a key cause of mortality associated with influenza?

    <p>A/H1N1</p> Signup and view all the answers

    Which strain of virus was the primary focus of the 2017/18 vaccination campaign in the UK?

    <p>A/H3N2</p> Signup and view all the answers

    Which influenza virus strain had a mortality rate of 33% in 1997?

    <p>H5N1</p> Signup and view all the answers

    Which influenza virus subtype was responsible for the 'Russian flu' in 1977?

    <p>H1N1</p> Signup and view all the answers

    Which of the following viruses has the potential to cause a pandemic and wipe out 30% of the world population?

    <p>H5N1</p> Signup and view all the answers

    What is the mechanism of action of Adamantanes against influenza A virus at low concentrations?

    <p>M2 ion channel blockage</p> Signup and view all the answers

    Influenza viruses are classified based on which surface glycoproteins?

    <p>Neuraminidase (NA) and Hemagglutinin (HA)</p> Signup and view all the answers

    What is the primary role of Neuraminidase (NA) during the influenza virus life cycle?

    <p>Release of viral progeny from infected cells</p> Signup and view all the answers

    Which type of sialic acid receptors do human influenza hemagglutinin molecules bind to?

    <p>α2,6-linked sialic acid</p> Signup and view all the answers

    Which influenza virus subtype was responsible for the 'Swine Flu' in 2009?

    <p>H1N1</p> Signup and view all the answers

    Which of the following influenza virus subtypes are the main epidemic strains?

    <p>H1N1 and H3N2</p> Signup and view all the answers

    Which of the following groups of individuals are strongly recommended for annual influenza immunization?

    <p>Individuals aged over 6 months with chronic conditions</p> Signup and view all the answers

    Which drug, approved in Japan and Korea in 2010, achieved FDA approval for the USA in December 2014?

    <p>Peramivir</p> Signup and view all the answers

    Which neuraminidase inhibitor is indicated for the treatment of acute uncomplicated influenza in patients who have been symptomatic for no more than 2 days?

    <p>Peramivir</p> Signup and view all the answers

    Which neuraminidase inhibitor is delivered via a Dry Powder Inhaler and marketed under the name 'Inavir'?

    <p>Laninamivir</p> Signup and view all the answers

    What was the primary reason for the IV version of Peramivir being on the market?

    <p>Issues with bioavailability</p> Signup and view all the answers

    What is a common side effect associated with the use of Peramivir?

    <p>Nausea</p> Signup and view all the answers

    Which neuraminidase inhibitor has a different route of delivery compared to others, involving inhalation via dry powder?

    <p>Zanamivir</p> Signup and view all the answers

    Which neuraminidase inhibitor is classified as a long-acting neuraminidase inhibitor with the trade name 'Inavir'?

    <p>Laninamivir</p> Signup and view all the answers

    'Rapiacta' is a neuraminidase inhibitor approved by Shionogi in which country?

    <p>'Japan'</p> Signup and view all the answers

    Which of the following antiviral drugs is NOT recommended by the CDC to treat flu during the 2023-24 season in the USA?

    <p>Ribavarin</p> Signup and view all the answers

    Which antiviral drug is no longer seeking regulatory approval in the UK for treating influenza?

    <p>Peramivir</p> Signup and view all the answers

    Which type of RdRp inhibitor is most promising due to its low cytotoxicity, high resistance barrier, and broad coverage of diverse RNA viruses?

    <p>PB1 or nucleoside analogue like inhibitors</p> Signup and view all the answers

    Which antiviral drug is approved for early treatment of flu in children aged 5 years to less than 12 years who do not have any chronic medical conditions?

    <p>Baloxavir marboxil</p> Signup and view all the answers

    Which antiviral drug is available as a pill or liquid suspension and is FDA approved for early treatment of flu in people 14 days and older?

    <p>Oseltamivir phosphate</p> Signup and view all the answers

    Which antiviral drug is no longer seeking regulatory approval in the UK for treating influenza due to the company informing NICE?

    <p>Peramivir</p> Signup and view all the answers

    Which antiviral drug is classified as a transition state inhibitor?

    <p>Zanamivir</p> Signup and view all the answers

    Which type of drug is associated with a disadvantage of converting Oseltamivir to GS4071 by esterases in the gastrointestinal tract for oral administration?

    <p>Neuraminidase inhibitors</p> Signup and view all the answers

    Which antiviral drug is a pill given as a single dose by mouth and is approved for early treatment of flu in all people aged 12 years and older?

    <p>Baloxavir marboxil</p> Signup and view all the answers

    Which antiviral drug is classified as a PB1 or nucleoside analogue like inhibitor?

    <p>Favipiravir</p> Signup and view all the answers

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