Opioid Antagonists: Uses and Effects

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Questions and Answers

Why might larger doses of opioid antagonists be required when administering them to patients who have used buprenorphine, butorphanol, nalbuphine or pentazocine?

  • These drugs inhibit the absorption of opioid antagonists, reducing their bioavailability.
  • These drugs have a higher binding affinity to opioid receptors, requiring more antagonist to displace them. (correct)
  • These drugs increase the rate of metabolism of opioid antagonists, reducing their effectiveness.
  • These drugs cause a paradoxical potentiation of opioid effects, necessitating a larger dose of antagonist.

Which of the following best describes why opioid antagonists are administered in cases of acute opioid overdose?

  • To directly neutralize the opioid molecule, rendering it inactive.
  • To temporarily block opioid receptors, reversing the adverse effect of opioid use. (correct)
  • To induce rapid metabolism of the opioid, thus lowering its concentration in the blood.
  • To permanently reverse the effects of opioids, ensuring no further opioid activity.

A patient recovering from surgery experiences reversed analgesia and central nervous system excitement. Which class of drugs is most likely responsible for these effects?

  • Opioid antagonists (correct)
  • Local anesthetics
  • Opioid agonists
  • Nonsteroidal anti-inflammatory drugs (NSAIDs)

What is the primary mechanism of action for opioid antagonists?

<p>They temporarily block opioid receptors, preventing opioid binding. (B)</p> Signup and view all the answers

A patient is being treated for opioid addiction with naltrexone. What is the intended effect of this medication?

<p>To reduce cravings and block the euphoric effects of opioids. (A)</p> Signup and view all the answers

Which of the following is a potential adverse effect associated with the use of opioid antagonists?

<p>Acute opioid abstinence syndrome (A)</p> Signup and view all the answers

Why is it important to recognize that opioid antagonists only temporarily block opioid receptors?

<p>To understand the need for potential repeat dosing, as the opioid effects may return. (D)</p> Signup and view all the answers

Which of the following opioid antagonists is commonly available as a nasal spray for emergency treatment of opioid overdose?

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

A patient with a history of chronic opioid use is given an opioid antagonist. What physiological response is most likely to occur?

<p>Rapid onset of withdrawal symptoms, CNS excitement and reversal of analgesia (A)</p> Signup and view all the answers

In which situation would methylnaltrexone, an opioid antagonist, be most appropriately used?

<p>To manage opioid-induced constipation without affecting central analgesia. (B)</p> Signup and view all the answers

Flashcards

Opioid Antagonists

Temporarily blocks opioid receptors and effects of the opioid. It does NOT reverse.

Opioid Antagonist - Indication

Reversal of the adverse effects of opioid use and is a treatment of acute opioid overdose.

Opioid Antagonist - Adverse Effects

Acute opioid abstinence syndrome, CNS excitement and reversal of analgesia especially common after surgery.

Opioid Antagonist - Names

Naloxone (NARCAN), Naltrexone, Nalmefene, Methylnaltrexone

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Study Notes

  • Opioid antagonists temporarily block opioid receptors and the effects of opioids, but do not reverse them.

Names

  • Naloxone (NARCAN) is an opioid antagonist.
  • Naltrexone is an opioid antagonist.
  • Nalmefene is an opioid antagonist.
  • Methylnaltrexone is an opioid antagonist.

Indications

  • Opioid antagonists can reverse the adverse effects of opioid use.
  • They are also used in the treatment of acute opioid overdose.

Adverse Effects

  • Opioid antagonists can cause acute opioid abstinence syndrome.
  • They may also cause CNS excitement and reversal of analgesia, especially after surgery.

Drug-Drug

  • Larger doses may be needed to reverse the effects of buprenorphine, butorphanol, nalbuphine, and pentazocine.
  • Naloxone HCl Nasal Spray (4mg) is an emergency treatment for opioid overdose.

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