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Anes. Pharm I Test 2
Opioid Agonist-Antagonist Drugs
| Question | Answer |
|---|---|
| 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
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