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Anes. Pharm I Test 2

Opioid Agonist-Antagonist Drugs

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