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Questions and Answers

What is the main goal of drug targeting?

  • Reduce the drug's potency
  • Increase the overall dose of the drug
  • Enhance the drug's toxicity
  • Direct the drug specifically to where its activity is desired (correct)

    • Why is targeting more difficult to achieve via the systemic route compared to local application?

  • Specific organs are more accessible locally
  • Specific organs are harder to reach systemically (correct)
  • Systemic route allows for easier targeting
  • Local delivery methods are more expensive

    • What is one of the key points of drug targeting mentioned in the text?

  • To have sustained activity at the site over the desired period (correct)
  • To increase drug toxicity
  • To reduce therapeutic profile
  • To cause immediate effects at the target site

    • Which type of targeting is mentioned as easy for local application in the text?

    <p>Targeting eye drops, inhalation powders, and skin creams</p> Signup and view all the answers

    How does drug targeting help in reducing toxicity?

    <p>By ensuring that drug activity is sustained over time at desired locations</p> Signup and view all the answers

    What is the primary requirement for a nanomaterial to be used in therapeutics?

    <p>It has to be essential for the therapeutic activity or confer unique properties to the drug</p> Signup and view all the answers

    What is the role of antibodies in drug delivery systems?

    <p>They recognize and attach to antigens as part of immune response</p> Signup and view all the answers

    What is the most abundant type of antibody produced in humans?

    <p>Immunoglobulin G (IgG)</p> Signup and view all the answers

    What type of endothelium has numerous gaps of varying sizes?

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

    Which of the following organs or tissues has a discontinuous endothelium?

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

    What is the primary mechanism by which passive targeting occurs?

    <p>Local physiological conditions</p> Signup and view all the answers

    Which of the following is an example of active targeting?

    <p>PEGylated liposome cancer therapy</p> Signup and view all the answers

    What is the size range of nanomaterials as defined in nanotechnology?

    <p>1-100 nm</p> Signup and view all the answers

    What is the primary role of nanomaterials in nanopharmaceuticals?

    <p>They are the pivotal therapeutic agent</p> Signup and view all the answers

    Which of the following is not a type of active targeting?

    <p>Passive targeting by MPS</p> Signup and view all the answers

    What is the primary mechanism by which nanoscience findings inform nanotechnology?

    <p>By controlling the physical properties of materials</p> Signup and view all the answers

    What role does the sub-endothelial basement membrane play in drug targeting?

    <p>It restricts the movement of macromolecules</p> Signup and view all the answers

    Which of the following is not a mode of drug targeting?

    <p>Chemical targeting</p> Signup and view all the answers

    What is the primary function of the Mononuclear Phagocytic System?

    <p>To remove foreign material such as bacteria and proteins</p> Signup and view all the answers

    Which of the following is NOT a requirement for an effective drug-targeting system?

    <p>Non-specific interactions with target tissues/organs</p> Signup and view all the answers

    What is the purpose of adding a hydrophilic polymer coat to a carrier system?

    <p>To reduce protein adsorption and opsonisation</p> Signup and view all the answers

    What is the process where the surface of a particle or pathogen is marked/coated by molecules for easier recognition and destruction by phagocytes?

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

    Which of the following is NOT a main type of delivery system for targeting drugs?

    <p>Soluble carrier system</p> Signup and view all the answers

    What is the primary factor influencing the clearance of particles by the Mononuclear Phagocytic System?

    <p>Particle size</p> Signup and view all the answers

    What is the role of opsonins in the process of phagocytosis?

    <p>They mark the surface of a particle or pathogen for easier recognition and destruction by phagocytes</p> Signup and view all the answers

    What is the purpose of a prodrug?

    <p>To improve the physicochemical properties of the drug for better targeting</p> Signup and view all the answers

    Which of the following is NOT a barrier to effective drug targeting?

    <p>The ability to deliver the drug to specific target site</p> Signup and view all the answers

    What is the purpose of the drug being retained over a suitable period at the target site once delivered?

    <p>To ensure the drug remains at the target site long enough to exert its therapeutic effect</p> Signup and view all the answers

    What is the main reason for the constant alteration of the antigenic structure of influenza A and B viruses?

    <p>To avoid detection by immune system</p> Signup and view all the answers

    Which enzyme is involved in synthesizing new genomes during replication of the influenza virus?

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

    What does the reassortment of genomic segments during co-infection lead to in the influenza virus?

    <p>Antigenic shift</p> Signup and view all the answers

    Why do RNA genomes mutate at a faster rate than DNA genomes during replication?

    <p>RNA polymerases have no proofreading ability</p> Signup and view all the answers

    Which component of the influenza virus acts as an antigen and is a target for vaccines?

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

    What is the main limitation of the H7N9 bird flu virus, according to the text?

    <p>Lack of human-to-human transmission</p> Signup and view all the answers

    Why does influenza virus evolution often require new vaccines to be produced every season?

    <p>To match the latest circulating strain</p> Signup and view all the answers

    What can lead to the production of a new virus subtype with altered virulence and tropism?

    <p>Genomic segment reassortment during co-infection</p> Signup and view all the answers

    Why is vaccination considered the preferred method for preventing flu, according to the text?

    <p>To protect against potential pandemics</p> Signup and view all the answers

    What contributes to losing protection from vaccines over time, as stated in the text?

    <p>Antigenic drift</p> Signup and view all the answers

    What is the primary role of neuraminidase (NA) in the infectious process?

    <p>Facilitate the fusion of viral membrane with the host cell membrane</p> Signup and view all the answers

    What is the rationale behind developing neuraminidase inhibitors as antiviral agents?

    <p>Neuraminidase has a structure that remains constant and differs from mammalian enzymes</p> Signup and view all the answers

    How did the discovery of the crystal structure of neuraminidase contribute to the development of antiviral agents?

    <p>Provided knowledge of the receptor that neuraminidase acts upon</p> Signup and view all the answers

    What was a significant challenge faced in developing analogues against resistant mutants to Amantadine?

    <p>Unsuccessful efforts in making analogues against resistant mutants</p> Signup and view all the answers

    Why did Rimantadine receive approval in 1993 as an antiviral agent for influenza?

    <p>It was less toxic than Amantadine and targeted both Influenza A and B</p> Signup and view all the answers

    What is the distinguishing feature between Adamantanes and Neuraminidase inhibitors?

    <p>Adamantanes prevent viral penetration, while Neuraminidase inhibitors target specific enzyme structures</p> Signup and view all the answers

    Which FDA-approved antiviral drug is recommended for early treatment of flu in children aged 5 years to less than 12 years, according to the text?

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

    Which antiviral drug is no longer seeking regulatory approval for treating influenza, as per the text?

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

    Which type of compounds is likely to be most promising in inhibiting RdRp of the influenza virus based on low cytotoxicity, high resistance barrier, and broad coverage of diverse RNA viruses?

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

    In the context of influenza virus evolution and drug resistance, what plays a critical role during the virus life cycle?

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

    Which therapeutic approach is suggested in the text to combat the potential of drug resistance in influenza viruses?

    <p>Practical synthesis of broad-spectrum antiviral drugs</p> Signup and view all the answers

    Which antibodies are mentioned in the text as potential therapeutics against human viral diseases?

    <p>Single-Domain Antibodies</p> Signup and view all the answers

    What is the primary function of RdRp during the early stages of infection by the influenza virus?

    <p>Synthesizing mRNA</p> Signup and view all the answers

    What is the mechanism of action of Oseltamivir as described in the text?

    <p>Binds to a specific active site of the virus</p> Signup and view all the answers

    Which amino acids are mentioned as interacting with the COO- group of Neu5Ac in the active site?

    <p>Arginine, Aspartate, Glutamine</p> Signup and view all the answers

    Why was Neu5Ac2en found to be inactive in vivo according to the text?

    <p>It lacks hydrogen bonds due to the absence of C-2 hydroxyl group</p> Signup and view all the answers

    What is the role of the glycerol side chain at C-6 in the active site?

    <p>Interacts with glutamate residues &amp; water by hydrogen bonds</p> Signup and view all the answers

    What was found to be a potential analogue at C-4 for Neu5Ac according to modeling studies?

    <p>$NH_2$</p> Signup and view all the answers

    What does Zanamivir (Relenza) primarily use to probe for hydrogen bonds in its interactions with the active site?

    <p>Ammonium nitrogen</p> Signup and view all the answers

    Why is Zanamivir considered selective and active in vivo according to the text?

    <p>$NH_2$ group forms more hydrogen bonds and vdw interactions</p> Signup and view all the answers

    What led to a 1000-fold increase in activity for Zanamivir compared to Neu5Ac2en?

    <p>$OH$ being replaced with an $NH_2$ at C-4</p> Signup and view all the answers

    Why is Zanamivir approved for influenza A & B despite its poor bioavailability?

    <p>$OH$ group at C-2 provides high affinity for influenza A NA</p> Signup and view all the answers

    What is one reason why Neu5Ac2en could not be used therapeutically according to the text?

    <p>$OH$ absent results in less hydrogen bonding causing inactivity in vivo</p> Signup and view all the answers

    What was the first FDA approval of a drug discovered by BioCryst Pharmaceuticals?

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

    Which neuraminidase inhibitor is approved for sale in Japan for the treatment of influenza and also for prevention (vaccine) since 2013?

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

    Which transition state inhibitor binds to both A & B forms and is known to be potent and highly selective?

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

    Which neuraminidase inhibitor has approval for sale in Europe from Merck KGa and Hikma, with the partner not yet announced?

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

    Which neuraminidase inhibitor is indicated for the treatment of acute uncomplicated influenza in patients 18 years and older who have been symptomatic for no more than 2 days?

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

    Which neuraminidase inhibitor is known to be just as effective as Zanamivir and Oseltamivir in in vitro tests but four orders of magnitude less active against mammalian & bacterial NAs?

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

    Which drug was developed to take advantage of both hydrophobic pockets and has the same relative stereochemistry as the 5-ring tetrahydrofuran (I)?

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

    Which drug has been identified as the most active structure among five-membered carbocycles and is suggested to have increased activity upon adding butyl to its structure?

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

    Which neuraminidase inhibitor had issues with bioavailability leading to an IV version being on the market despite confirmation of oral bioavailability?

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

    Which neuraminidase inhibitor achieved similar activity to Neu5Ac2en through different positioning of its ring in the active site?

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

    Which of the following is NOT a limitation of current anti-viral therapeutic agents against influenza?

    <p>High toxicity</p> Signup and view all the answers

    Which of the following statements about neuraminidase inhibitors is FALSE?

    <p>They are effective against all strains of the influenza virus</p> Signup and view all the answers

    What is the primary role of the influenza virus's hemagglutinin protein?

    <p>Facilitating the entry of the virus into host cells</p> Signup and view all the answers

    Which of the following is NOT a treatment or prevention strategy for influenza?

    <p>Administration of interferon-alpha</p> Signup and view all the answers

    Which of the following is NOT a characteristic of the neuraminidase protein of the influenza virus?

    <p>It plays a role in facilitating the entry of the virus into host cells</p> Signup and view all the answers

    Which type of influenza virus poses the greatest concern as a human pathogen?

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

    What is the main function of neuraminidase in the influenza virus's life cycle?

    <p>Cleaving the terminal Neu5Ac to degrade the mucus layer</p> Signup and view all the answers

    Which type of influenza virus can bind to both alpha-2-3 and alpha-2-6 sialic acid receptors?

    <p>Swine influenza</p> Signup and view all the answers

    What is the genetic material of the influenza virus?

    <p>Single-stranded RNA (negative sense)</p> Signup and view all the answers

    Which viral surface glycoprotein is responsible for binding the virus to the cell being infected?

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

    What is the main cause of mortality in influenza infections, especially in the elderly and those with weak immune systems?

    <p>Infection in the epithelial cells of the upper respiratory tract</p> Signup and view all the answers

    Which type of influenza virus is responsible for the H1N1 swine flu?

    <p>Influenza virus A</p> Signup and view all the answers

    What is the primary function of haemagglutinin in the influenza virus's life cycle?

    <p>Interacting with host cell membrane to allow adsorption</p> Signup and view all the answers

    What is the main function of neuraminidase inhibitors in the treatment of influenza infections?

    <p>Inhibiting the release of virion progeny from infected cells</p> Signup and view all the answers

    Which type of sialic acid receptor is preferentially bound by avian influenza viruses?

    <p>Alpha-2-3 sialic acid receptors</p> Signup and view all the answers

    Which strain of the influenza virus was included in the 2017/18 vaccine to provide protection against a fourth B strain?

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

    Which age group is recommended to receive the live influenza vaccine (Fluenz Tetra®) unless contra-indicated?

    <p>Children aged 2–17 years</p> Signup and view all the answers

    Which strain of the influenza virus was contained in the 2017/18 vaccine to protect against the A/H3N2 strain?

    <p>A/Hong Kong/4801/2014 (H3N2)-like virus</p> Signup and view all the answers

    Which of the following groups was recommended to receive the seasonal influenza vaccine in the 2017/18 national influenza immunisation programme?

    <p>All children aged 2–8 years on 31 August 2017</p> Signup and view all the answers

    Which of the following strains of the influenza virus is particularly associated with affecting children?

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

    Which of the following statements best describes the role of the World Health Organization (WHO) in the development of influenza vaccines?

    <p>The WHO recommends the strains of influenza virus to be included in vaccines</p> Signup and view all the answers

    Which of the following statements best describes the production process of the influenza vaccine?

    <p>The production process of the influenza vaccine starts in February and is completed in August</p> Signup and view all the answers

    Which of the following viruses has been reported to cause human infections in China in 2021?

    <p>H5N6</p> Signup and view all the answers

    Which of the following regions has reported the largest outbreak of avian influenza in 2021?

    <p>Northern Ireland</p> Signup and view all the answers

    Which of the following statements best describes the role of children in the spread of influenza virus?

    <p>Children are regarded as 'super-spreaders' of the influenza virus</p> Signup and view all the answers

    Which of the following modifications resulted in a significant increase in activity for 6-carboxamides?

    <p>Changing stereochemistry at C-4</p> Signup and view all the answers

    Which structural modification of the 6-carboxamides led to the development of carbocyclics?

    <p>Replacing the ring oxygen with a methylene group</p> Signup and view all the answers

    Which modification of Structure II resulted in a significant increase in potency?

    <p>Introducing a hydroxyl group in place of the side chain</p> Signup and view all the answers

    Which alkyl ether was found to have the highest activity among the linear chain alkyl ethers?

    <p>Propyl ether</p> Signup and view all the answers

    Which modification of the glycerol side chain led to an increase in binding interactions?

    <p>Replacing the glycerol side chain with an alkyl ether</p> Signup and view all the answers

    Which structural modification of carbocyclics was found to be the most potent?

    <p>Introducing a hydroxyl group in place of the side chain</p> Signup and view all the answers

    Which modification of the carboxyl group in the carbocyclics resulted in the most potent structure?

    <p>Introducing a hydroxyl group in place of the side chain</p> Signup and view all the answers

    Which modification of the glycerol side chain in the carbocyclics resulted in a decrease in polarity?

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

    Which modification of the carboxyl group in the carbocyclics resulted in a decrease in polarity?

    <p>Replacing the carboxyl group with an amino group</p> Signup and view all the answers

    Which modification of the glycerol side chain in the carbocyclics resulted in an increase in binding interactions?

    <p>Modifying the glycerol side chain with branching</p> Signup and view all the answers

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