Opioid Agonist-Antagonist Drugs
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| What is a competitive antagonist? | a drug that reversibly binds to receptor at the same site as the agonist but does NOT activate the receptor
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| What is a non-competitive antagonist? | a drug that irreversibly binds to receptor at a separate site from the agonist and disable that receptor
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| What is a partial agonist? | a drug that has a high affinity for the receptor but not as much intrinsic activity
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| What is a superagonist? | a drug that has greater effects at the receptor than the defining receptor agonist; example = fentanyl 100x more potent at mu receptor than morphine
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| What is an agonist-antagonist? | a drug with a mixed composition of agonist and antagonist effects; may be partial or full agonism
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| Opioids that have antagonist effects on which 2 receptor types are useful in pain management? | mu and kappa
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| Do opioid agonist-antagonist drugs have an effect on intrabiliary pressure? | No
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| True or false: subsequent doses of agonist after opioid agonist-antoagonist administration may NOT provide adequate analgesia | True
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| What can antagonism of Mu opioid receptors lead to? | withdrawal
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| The undesirable psychotomimetic effects caused by opioid agonist-antagonist drugs are suggested to be associated with which opioid receptor? | kappa
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| What are the psychotomimetic effects caused by opioid agonist-antagonist drugs? | dysphoria, confusion (especially in elderly), depression, NO euphoria
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| Which receptors does Pentazocine (Talwin) antagonize and agonize? | a weak antagonist of mu receptors and a partial kappa agonist
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| Does Pentazocine (Talwin) antagonize respiratory depression? | no
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| What are 2 indication for the use of Pentazocine (Talwin)? | relief of moderate pain; chronic pain with increased risk of physical dependence
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| What are 3 effects of Pentazocine (Talwin)? | analgesia, sedation, mild respiratory depression
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| What are the CV side effects of Pentazocine (Talwin)? | increased HR & cardiac workload; increased SBP and PAP; increased myocardial O2 consumption
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| What are the non CV side effects of Pentazocine (Talwin)? | sedation, dysphoria, diaphoresis, dizziness, dissociation, hallucinations, fetal depression
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| True or false: Butorphanol (Stadol) causes analgesia more potent than morphine | True
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| What are three indications for Butorphanol (Stadol)? | post-op pain, migraine headaches, post-op shivering
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| What are the effects of Butorphanol (Stadol)? | analgesia and respiratory depression
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| What are the side effects of Butorphanol (Stadol)? | sedation, nausea, diaphoresis, respiratory depression, dissociation, increased CO and workload, increased SBP and PAP
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| Nalbuphine (Nubain) has a potency comparable to __________ | morphine
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| Which receptors does Nalbuphine (Nubain) antagonize? Agonize? | Mu receptor antagonist; kappa receptor agonist
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| Which agonist-antagonist drug is useful in antagonizing pruritus induced by epidural morphine? | Nalbuphine (Nubain)
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| Which agonist-antagonist drugs are useful in reversing lingering fentanyl-induced respiratory dress ion while providing analgesia? | Nalbuphine (Nubain); Buprenorphine (Buprenex)
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| Does Nalbuphine (Nubain) have any CV side effects? | No
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| What are 2 indications for Buprenorphine (Buprenex)? | moderate ro severe cancer pain; opioid dependence
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| Buprenorphine (Buprenex) has mu receptor affinity 50x greater than _______ | morphine
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| Which agonist-antagonist drug is resistant to antagonism by narcan? | Buprenorphine (Buprenex)
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| Which agonist-antagonist drug has a prolonged duration of up to 8 hours? | Buprenorphine (Burprenex)
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| Which receptors does Buprenorphine (Buprenex) agonize? Antagonize? | partial mu receptor agonist; antagonizes mu receptors as well
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Created by:
Mary Beth
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