Mixed Agonists/Antagonists and Antagonists – Opioid Analgesics

by Pravin Shukle, MD

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    Let's move on to the mixed agonists, antagonists class of drugs. So, these are harder to understand, but this is where the receptors start to come into play. Let's talk about Nubain. Now, Nubain will not antagonize other opioid drugs. It may still be addictive however. It is an agonist at the kappa receptor and an antagonist at the mu receptor. What this gives us is a "respiratory ceiling". So, what that means is, is that even if you give very high doses of this drug, there is minimal risk of respiratory depression. There is also a lower risk of addiction. And in fact, this particular agent was taken off the class II list of controlled substances by the FDA. It is also used for morphine induced itching or pruritus, so that you don't get as many histamine reactions from this medication. Now, you're unlikely to be tested on this drug, at least in the past, I don't know if this is going to be on the exams in the future, it's relatively new, it is something that we're starting to use more and more in clinical practice. So although it hasn't been tested on extensively in the past, just be aware of it and keep your eyes and ears open. Now, this is another morphine analogue. It is a semisynthetic partial agonist. Uses are in opioid addiction with methadone, for use in some pain management patients, it is found to be effective in refractory depression as well, and there is a particular condition called neonatal abstinence syndrome. This is why this drug is on our list because it is used in those patients who are neonates, who are survivors of mothers who are addicted to morphine. It is currently being studied, by the time you're watching this video, the...

    About the Lecture

    The lecture Mixed Agonists/Antagonists and Antagonists – Opioid Analgesics by Pravin Shukle, MD is from the course CNS - Pharmacology. It contains the following chapters:

    • Opioid Analgesics - Mixed Agonists/Antagonists
    • Opioid Analgesics - Antagonists

    Included Quiz Questions

    1. Its agonist/antagonist receptor activity
    2. Only reacts with kappa opioid receptors
    3. It only antagonizes mu opioid receptors
    4. This medication only acts peripherally, protecting the central nervous system
    5. Its very short half life reduces risk of overdosing
    1. Buprenorphine prevents use of other, stronger opioids because of its strong binding affinity
    2. Buprenorphine is very addictive and should not be prescribed in any patient with a history of substance abuse.
    3. Using buprenorphine with muscarinic agonists contraindicated due to risk of overdose and respiratory depression.
    4. Buprenorphine is a class D teratogen and should not be prescribed to pregnant patients, in patients attempting to get pregnant, or lactating mothers.
    5. Buprenorphine causes cholestasis in newborns and should not be used in this population.
    1. Hallucination
    2. Sweating
    3. Improved spontaneous respiration
    4. Placebo pain
    5. Improved mentation
    1. Buprenorphine
    2. Naloxone
    3. Oxycontin at a lower dosage
    4. Fentanyl patch
    5. Nicotine patch

    Author of lecture Mixed Agonists/Antagonists and Antagonists – Opioid Analgesics

     Pravin Shukle, MD

    Pravin Shukle, MD

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