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

What is the primary mechanism of action of naltrexone?

<p>Opioid antagonist (D)</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 (B)</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 (A)</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 (C)</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 (B)</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 (A)</p> Signup and view all the answers

What is the primary use of diphenoxylate?

<p>As an antidiarrheal agent (B)</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 (B)</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 (B)</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 (D)</p> Signup and view all the answers

What is the class of opioid receptors?

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

What is the effect of activating the opioid receptor?

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

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

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

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