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Analgesics

QuestionAnswer
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
 

 



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