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Agonist/Antagonists
Pharm (Test 2)
| Question | Answer |
|---|---|
| Describe the receptor affinity of Pentazocine (Talwin). | weak mu antagonist, partial kappa agonist |
| What are the indications for Pentazocine (Talwin)? | moderate pain, chronic pain, inc. risk of physical dependence |
| What are the effects of Pentazocine (Talwin)? | analgesia, sedation, mild resp. depression |
| Describe the CV effects of Pentazocine (Talwin). | inc. HR, cardiac workload, SBP, PA pressure, and myocardial O2 consumption |
| What patients have special considerations for the use of Pentazocine (Talwin)? | IHD, CHF, MI, pregnant mothers |
| Does narcan antagonize Pentazocine (Talwin)? | yes |
| Does Pentazocine (Talwin) antagonize resp. depression? | no |
| Describe the receptor affinity of Butorphanol (Stadol). | more kappa than mu or sigma |
| Compare potency between Talwin and Stadol. | Stadol is 20X more agonist potent and 10-30X more antagonist potent than Talwin |
| Compare analgesic potency between Butrophanol (Stadol) and morphine. | stadol has more analgesic potency than morphine |
| What are the indications of Butrophanol (Stadol)? | post-op pain, migraine headaches, post-op shivering |
| What are the effects of Butrophanol (Stadol)? | analgesia, resp. depression |
| What are some side effects of Pentazocine (Talwin)? | (DD) sedation, dysphoria, diaphoresis, dizziness, dissociation, "weird" feelings, hallucinations, NO mood elevation |
| What are some side effects of Butorphanol (Stadol)? | withdrawal after d/c, sedation, nausea, diaphoresis, resp. depression, dissociation, dysphoria is RARE |
| Describe the CV concerns with Butrophanol (Stadol). | inc. CO, cardiac workload, SBP and PA pressure |
| What patients have special considerations for the use of Butrophanol (Stadol)? | CHF and MI pts |
| Which agonist/antagonist has a nasal spray? | Stadol |
| Describe the receptor affinity of Nalbuphine (Nubain). | mu antagonist, kappa agonist |
| Compare the potency of Nalbuphine (Nubain) to morphine. | very comparable |
| What are the indications for use of Nalbuphine (Nubain)? | reversing fent-induced resp. dep; antagonizes pruritis induced by epidural morphine |
| What are the effects of Nalbuphine (Nubain)? | kappa provide adequate pain relief w/ less resp. depression, analgesia, sedation |
| What are the side effects of Nalbuphine (Nubain)? | withdrawal after d/c, diaphoresis, headache, dissociation |
| Describe the CV concerns for Nalbuphine (Nubain). | none |
| Does narcan antagonize stadol? | no |
| Does narcan antagonize Nubain? | yes |
| True or False: Nalbuphine (Nubain) has a ceiling for respiratory depression. | True |
| Describe the receptor affinity of Buprenorphine (Buprenex). | partial mu agonist, mu antagonist |
| Describe the receptor affinity of Buprenorphine (Buprenex) to that of morphine. | Buprenex's affinity for mu receptor is 50X greater than morphine |
| What are the indications for use of Buprenorphine (Buprenex)? | reversing fent-induced resp. dep; effective on moderate to severe cancer pain; opioid dependence |
| What are some side effects of Buprenorphine (Buprenex)? | withdrawal after d/c, sedation, n/v, diaphoresis, headache, dizziness |
| Does narcan antagonist Buprenorphine (Buprenex)? | no |
| Which a/a can treat migraine headaches? | stadol |
| Which a/a(s) can be used to treat fent-induced resp. dep? | nubain, buprenex |
| Which a/a(s) can cause withdrawal after d/c? | stadol, nubain, buprenex |
| Which a/a(s) cause inc. HR, SBP, cardiac workload, etc? | talwin, stadol |
| Which a/a(s) can be antagonized by narcan? | talwin, nubain |
| Which a/a is available in a nasal spray? | stadol |
| Which a/a has a potency comparable to morphine? | nubain |
| Which a/a has a ceiling resp. depressant effect? | nubain |
| Which a/a can cross the placental barrier and cause fetal depression? | talwin |
| Which a/a(s) are kappa agonists? | talwin, stadol, nubain |
| Which a/a can cause "weird" feelings and hallucinations? | talwin |
| Which a/a is effective for cancer pain? | buprenex |
| Which a/a has a mu receptor affinity 50X greater than morphine? | buprenex |
| Which a/a has analgesic potency greater than morphine? | stadol |
| Which a/a can be used to treat post-op shivering? | stadol |
| Which a/a antagonizes the pruritis induced by epidural morphine? | nubain |