Opioid Analgesics

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  1. morphine
    • opioid agonist
    • renal excretion (phase II - glucuronidation)
    • metabolites: M6G (5-10%, 10x more potent), M3G (70-80%, no analgesia)
  2. hydromorphone
    • opioid agonist
    • renal excretion (phase II - glucuronidation)
    • metabolites: H6G, H3G
  3. fentanyl
    • opioid agonist
    • hepatic metabolism (CYP3A4)
  4. oxycodone
    • opioid agonist
    • hepatic metabolism (CYP2D6, CYP3A4)
    • active metabolites
  5. naloxone
    • competitive antagonist at MOR, DOR, KOR with high affinity for MOR but no efficacy
    • no oral absorption, but mixed with oral opioid as abuse deterrent, blocks MOR in gut
    • IV or IM blocks peripheral and central MOR
    • onset within seconds, very short half-life
  6. naltrexone
    • competitive antagonist at MOR, DOR, KOR with high affinity for MOR but no efficacy
    • oral, longer duration of action
    • new long-acting IM depot product for opioid or alcohol addiction
  7. buprenorphine
    • high affinity, partial agonist for MOR
    • initial opioid response, but plateaus
    • ceiling effect on analgesia and resp depression
    • long dissociation - used for opioid addiction (w or w/o naloxone)
    • may precipitate withdraw if added to full agonist
  8. Tramadol
    • weak opioid agonist (MOR)
    • serotonin and NE reuptake inhibitor
  9. nalbuphine
    • agonist-antagonist
    • high MOR affinity, poor MOR efficacy to the point of possible antagonist activity
    • KOR agonist
    • complex usage

Card Set Information

Author:
jboi
ID:
323350
Filename:
Opioid Analgesics
Updated:
2016-09-20 03:05:09
Tags:
MOHD4 opioid analgesics pharmacology
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Description:
MOHD 4 lecture 53
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