17 Questions
What is the approximate analgesic potency of propoxyphene compared to morphine?
1/10th
What is the main concern with the metabolism of propoxyphene?
It results in naloxone-insensitive cardiotoxicity
What is the approximate percentage of tramadol's analgesic effect that is antagonized by naloxone?
30%
What is the difference in potency between the (+) and (-) enantiomers of tramadol?
The (+) enantiomer is 30 times more potent
What is the primary mechanism of action of naltrexone?
Opioid antagonist
What is the duration of action of naltrexone after a single dose of 50 mg?
24 hours
What is the analgesic potency of a 50-mg dose of pentazocine compared to codeine?
Equal to 60 mg of codeine
What is the purpose of including naloxone in the pentazocine tablet?
To deter drug abuse by making injection difficult
What is the result of structural simplification of the benzomorphan ring system?
Formation of a flexible ring structure
What is the characteristic of meperidine that indicates its analgesic activity?
It causes the Straub tail reaction in mice
What is the primary use of diphenoxylate?
As an antidiarrheal agent
What is the effect of adding an electron withdrawing, lipophilic substituent in the para position of Phe4 on the activity?
It greatly increases the activity
Which position of the peptide appears to tolerate more residue changes than the other positions?
Position 5
What is the result of the loss of the fifth residue to yield the tetrapeptide Tyr1-Gly2-Gly3-Phe4?
It maintains weak activity
What is the class of opioid receptors?
G-protein–coupled receptor
What is the effect of activating the opioid receptor?
It inhibits the activity of adenylate cyclase
What is the full form of MOP in opioid receptor subtypes?
Mu for morphine
Test your knowledge of the pharmacological properties of propoxyphene and tramadol, including their analgesic potency, metabolism, and adverse effects. Learn about the mechanisms of action and potential dangers of these opioids.
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