MSOP1016 The Science of Medicine 3: The Opioid Analgesics Lecture 4&5 Quiz
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Questions and Answers

What does the term 'opium' mean in Greek?

  • Water
  • Seeds
  • Juice (correct)
  • Herbal remedy
  • In medicinal chemistry, what is the purpose of drug design strategies like extension and simplification of structure?

  • To prevent interaction with opioid receptors
  • To increase side effects
  • To develop various morphine analogues (correct)
  • To decrease analgesic activity
  • What is the main focus of discussing the Stereochemistry of opioid analgesics?

  • Receptor binding specificity (correct)
  • Application of drug design strategies
  • Functional groups for analgesic activity
  • Structural features of morphine
  • Why are analogues like Morphinans and Benzomorphans considered important in the study of opioid analgesics?

    <p>To enhance receptor interaction</p> Signup and view all the answers

    What key aspect of morphine's structure do medicinal chemists aim to understand?

    <p>Its structural features</p> Signup and view all the answers

    What is the significance of rigidification in developing opioids like buprenorphine?

    <p>To increase receptor selectivity</p> Signup and view all the answers

    What is the correct structural feature of morphine that enables it to bind through various interactions?

    <p>Functional groups capable of forming ionic, hydrogen bond, and van der Waals interactions</p> Signup and view all the answers

    In the context of opioid analgesics, what is the significance of morphine being poorly absorbed orally?

    <p>It limits its potential clinical use</p> Signup and view all the answers

    What are the common side effects associated with the use of morphine?

    <p>Respiratory depression and constipation</p> Signup and view all the answers

    How does codeine differ from morphine in terms of its analgesic activity?

    <p>Codeine is less active when injected peripherally than when it crosses the blood-brain barrier</p> Signup and view all the answers

    What distinguishes heroin from morphine in terms of crossing the blood-brain barrier?

    <p>Heroin can directly cross the blood-brain barrier</p> Signup and view all the answers

    Why is it essential to test analogues for activity when studying structure-activity relationships?

    <p>To determine the importance of functional groups for activity</p> Signup and view all the answers

    Which molecule is used as a substitute for morphine or heroin to treat addicts?

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

    Which form of methadone has 2 times the activity of morphine?

    <p>R form</p> Signup and view all the answers

    Which molecule uses a flexible binding mode different from morphine?

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

    Which opioid displays properties of being an antagonist with agonist properties?

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

    Which opioid has the property of dissociating slowly from the receptor?

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

    What is the main advantage of simplifying drug analogues according to the text?

    <p>Decrease production cost</p> Signup and view all the answers

    Which functional group is removed to create a series of tetracyclic compounds known as morphinans?

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

    What change in the structure of N-methylmorphinan increased its potency compared to morphine?

    <p>Removal of ring D</p> Signup and view all the answers

    Which compound has the same analgesic activity as morphine after removing both rings C and D?

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

    What impact did replacing the N-methyl group of metazocine with a phenyl group have on phenazocine?

    <p>Increased potency without addiction properties</p> Signup and view all the answers

    What is a key characteristic of pentazocine in terms of addiction potential?

    <p>Low addiction risk</p> Signup and view all the answers

    What distinguishes bremazocine from pentazocine in terms of activity?

    <p>Higher potency than morphine</p> Signup and view all the answers

    What is the main drawback of Pethidine compared to Methadone?

    <p>Greater dependence potential</p> Signup and view all the answers

    What is the primary advantage of benzomorphans over morphine according to the text?

    <p>Rapid onset and long duration</p> Signup and view all the answers

    What is an important clinical benefit of benzomorphans?

    <p>Balance analgesic benefits with lower addiction/tolerance risks</p> Signup and view all the answers

    Which functional group is indicated as the most important for the analgesic activity of morphine in the given text?

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

    What effect is observed on the analgesic activity of analogues if the 3-OH group in morphine is modified?

    <p>Activity decreases significantly</p> Signup and view all the answers

    Which receptor is identified as the main one for both analgesic effects and side effects of morphine in the text?

    <p>Mu (µ)</p> Signup and view all the answers

    What is the biologically active enantiomer of morphine with regard to its stereochemistry?

    <p>(5R, 6S, 9R, 13S, 14R)</p> Signup and view all the answers

    What is the strategy involved in drug design focused on extending a lead compound by adding extra functional groups to probe for additional binding regions?

    <p>Drug extension</p> Signup and view all the answers

    What effect does increasing the alkyl group size attached to the nitrogen atom from methyl to butyl have on agonist activity according to the text?

    <p>Decreases agonist activity to zero</p> Signup and view all the answers

    Which type of drug antagonist binds to analgesic receptors without activating them and blocks morphine binding?

    <p>Pure antagonist</p> Signup and view all the answers

    In drug extension at the N-atom of morphine, which additional groups lead to naloxone, naltrexone, and nalorphine?

    <p>Allyl or propyl groups</p> Signup and view all the answers

    What is the main purpose of opioid drug design mentioned in the text?

    <p>To minimize side effects</p> Signup and view all the answers

    Which group indicated in drug extension for morphine increases activity by 14-fold according to the text?

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

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