Pharm

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Author:
shirljoa
ID:
214610
Filename:
Pharm
Updated:
2013-04-20 22:34:15
Tags:
opioids
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Description:
Opioids
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  1. Morphine
    • - Natural Alkaloid Papaver somniferum
    • - acts primarily on mu repectors (some k)
    • - rapid tolerance
    • - Activity set at 1
    • - uses: mainly analgesic
  2. Heroin
    • -Diacetylmorphine
    • - semisynthetic, easily prepared from morphine
    • - 2x aspotent as morphine, but more lipid soluble
    • - enters CNS rapidly, causing quick euphoria
    • -High addiction liability
  3. Codeine
    • - 1/10 analgesic potency of morphine
    • - < addiction or resp depression
    • - partially converted to morphine in body
    • - potent antitussive in parent form
  4. Oxycodone (oxycontin)
    • - 2x as potent as morphine (analgesia)
    • - high euphoria
    • - avail in 160 mg ER tab
    • - deaths associated w/ chewing ER form
  5. Levorphanol
    • - 5x potency of morphine (analgesic)
    • - less constipating
    • - longer lasting
  6. Dextrometorphan (Bromfed-DM)
    • - D-isomer (no analgesic activity)
    • - effective antitussive
  7. Meperidine (Demerol)
    • -1/10 the mg potency of morphine (analgesic) & shorter duration of action
    • - no miosis, thus freq abused d/t hard to detect
    • - metabolized to normeperidine (CNS stimulant)
    • - Contraindicated w/ MAOI therapy
  8. Propoxyphene (Darvon)
    • -structurally related to methadone, < 1/10 potency per mg
    • - D/C'ed
  9. Fentanyl (Sublimaze)
    • - chemically releated to meperidine
    • - 80x as potent (analgesic) as morphine
    • - short 1/2 life of redistribution (12.5 min)
  10. Remifentanyl (Ultiva)
    • -selective mu receptor agonist
    • - has ester linkage (hydrolysis by non-specific esterases
    • - used as adjunct for induction and/or maintainence in ped pts
  11. Etorphin (Immobilon)
    • - Veterinary use only
    • - 1000x morphine potency
    • - large animal immobilizer
    • - toxic to humans
  12. Buprenorphine (Buprenex)
    • - partial opioid agonist
    • - binds mu receptors  (elicits weaker max response than other agonists)
    • - less abuse potential
    • - used to counteract heroin and morphine addiction w/o causing full-blown w/drawal sx
  13. Nalorphine (Nalline)
    • - agonist/antagonist
    • - US vet use only
    • - mu receptor antagonist (blocks analgesia & euphoria)
    • - weak k agonist (stimulates analgesia & sedation)
    • - large doses may cause dysphoria and hallucinations
  14. Tramadol (Ultram)
    • - parent and active metabolite have weak affinity for mu receptors
    • - analgesic effect not entirely reversed by narcan
    • blocks re-uptake of serotonin & NE
    • -sx: dizziness, sedation, seizures & hallucination

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