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Analgesics
| Question | Answer |
|---|---|
| Opioid receptors | mu, delta, kappa |
| Mu receptor | when activated by opioid analgesics, promotes analgesia, respiratory depression, euphoria, and sedation |
| Kappa receptor | when activated by opioid analgesic, causes analgesia and sedation, and some psychomimetic effects |
| Opioid agonists | Fentanyl, Methadone, Meperidine, Codeine, Oxycodone, Vicodin, Propoxyphene |
| Fentanyl [sublimaze] | parenteral opioid agonist that is used for surgical anesthesia |
| Fentanyl [duragesic] | transdermal opioid agonist analgesic |
| Fentanyl [Actiq] | opioid agonist that is used as a lozenge stick for breakthrough cancer pain |
| Methadone | opioid agonist used in drug treatment programs, but has S/E of QT prolongation |
| Torsades de pointes | consequence of QT prolongation |
| Codeine | used for mild/moderate pain, very good cough suppressant |
| Oxycodone [Percocet, Oxycontin] | opioid agonist with analgesia that equals codeine; used in combined with ASA, acetaminophen, and ibuprophen |
| Agonist/antagonist opioids | act as agonist at kappa receptors, but antagonists at mu receptors. These have a lower potential for abuse, and have less respiratory depression. When given in pts w/ addiction to pure opioid agonists, they precipitate a withdrawal syndrome |
| Agonist/antagonist opioids | Pentazocine, Butorphanol [Stadol], nalbuphine [Nubain], Buprenorphine |
| Pentazocine | Agonist/antagonist opioid whose S/E increases cardiac workload |
| Pentazocine | Agonist/antagonist opioid that has a ceiling respiratory depression |
| Butorphanol | Agonist/antagonist opioid that acts like pentazocine |
| nalbuphine [Nubain] | Agonist/antagonist opioid that has ceiling analgesia as well as ceiling respiratory depression; give small doses b/c physical dependence may develop |
| Buprenorphine[Buprenex] | Agonist/antagonist opioid whosem analgesic action = morphine, but there is no risk for tolerance or respiratory depression, but it may precipitate a withdrawal rxn in pts dependent on pure opioid agonists |
| PCA | Commonly uses morphine to provide a greater protection against ain recurrence |
| Opioid Antagonists | used mainly as an antidote for opioid overdose, reversal of respiratory depression (post-op), and management of opioid addiction |
| Opioid antagonists | Naloxone[Narcan], Naltrexone, Nalmefene |
| Naloxone[Narcan] | structural analog of morphine used to reverse respiratory depression, as well as management for opioid addiction |
| Natrexone | Opioid antagonist that is used for tx of opioid and alcohol abuse, but it doesn't suppress opioid cravings; this drug may have failed compliance issues |
| Nalmefene | long-acting naltrexone analog w/ long 1/ life, used for reversal of post-op opioid effects |
| Centrally-acting non-opioid analgesics | Tramadol, Clonidine, Ziconotide |
| TramaCentrally-acting non-opioid analgesicsdol | Codeine analog used for mod/severe pain relief; has weak agonist effects at mu receptors |
| Clonidine [duraclon] | Centrally-acting non-opioid epidural analgesic for severe pain relief |
| Clonidine [Catapres] | PO or transdermal Centrally-acting non-opioid analgesic that is approved for hypertension treatment |
| Ziconotide | intrathecal Centrally-acting non-opioid analgesic that does not act at opioid receptors; it is a selective antagonist @ N-type Ca2+ channels on neurons to promote relief of severe pain |
| Morphine | Pure opioid agonist that may be used for tx of MI; S/E: respiratory depression |
| Tolerance | when increased doses of a drug is needed to achieve the same effect of a lower dose |
| Strong opioid Agonists | Morphine, fentanyl, methadone, sufentanyl, meperidine |
| Mod/Strong opioid Agonists | Codeine, oxycodone, hydrocodone, propoxyphene |
| Codeine | similar to morphine in effects, but produce less analgesia, potential for abuse, and respiratory depression; used for mild/mod pain and as a cough suppressant |
| Narcan | structural analog of codeine that acts as a competitive antagonist @ opioid receptors; acts to revers pure opioid overdose. Main S/E: withdrawal sx and reversal of analgesia |
| Clonidine | centrally acting non-opioid analgesic that relieves pain by binding pre/post-synaptic alpha 2 receptors |
| Tramadol | centrally acting non-opioid analgesic that relieves pain by blocking uptake of NE and 5HT |
Created by:
corpilla