Pharmacology of Opioids: Propoxyphene and Tramadol
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Questions and Answers

What is the approximate analgesic potency of propoxyphene compared to morphine?

  • 1/10th (correct)
  • 1/2
  • 1/5th
  • Equal
  • What is the main concern with the metabolism of propoxyphene?

  • It results in naloxone-insensitive cardiotoxicity (correct)
  • It causes respiratory depression
  • It leads to increased analgesic potency
  • It increases the risk of addiction
  • What is the approximate percentage of tramadol's analgesic effect that is antagonized by naloxone?

  • 40%
  • 20%
  • 30% (correct)
  • 10%
  • What is the difference in potency between the (+) and (-) enantiomers of tramadol?

    <p>The (+) enantiomer is 30 times more potent</p> Signup and view all the answers

    What is the primary mechanism of action of naltrexone?

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

    What is the duration of action of naltrexone after a single dose of 50 mg?

    <p>24 hours</p> Signup and view all the answers

    What is the analgesic potency of a 50-mg dose of pentazocine compared to codeine?

    <p>Equal to 60 mg of codeine</p> Signup and view all the answers

    What is the purpose of including naloxone in the pentazocine tablet?

    <p>To deter drug abuse by making injection difficult</p> Signup and view all the answers

    What is the result of structural simplification of the benzomorphan ring system?

    <p>Formation of a flexible ring structure</p> Signup and view all the answers

    What is the characteristic of meperidine that indicates its analgesic activity?

    <p>It causes the Straub tail reaction in mice</p> Signup and view all the answers

    What is the primary use of diphenoxylate?

    <p>As an antidiarrheal agent</p> Signup and view all the answers

    What is the effect of adding an electron withdrawing, lipophilic substituent in the para position of Phe4 on the activity?

    <p>It greatly increases the activity</p> Signup and view all the answers

    Which position of the peptide appears to tolerate more residue changes than the other positions?

    <p>Position 5</p> Signup and view all the answers

    What is the result of the loss of the fifth residue to yield the tetrapeptide Tyr1-Gly2-Gly3-Phe4?

    <p>It maintains weak activity</p> Signup and view all the answers

    What is the class of opioid receptors?

    <p>G-protein–coupled receptor</p> Signup and view all the answers

    What is the effect of activating the opioid receptor?

    <p>It inhibits the activity of adenylate cyclase</p> Signup and view all the answers

    What is the full form of MOP in opioid receptor subtypes?

    <p>Mu for morphine</p> Signup and view all the answers

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