Opioid/Opiates

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Author:
mp
ID:
205449
Filename:
Opioid/Opiates
Updated:
2013-03-06 16:59:07
Tags:
Pharmacology II Opioid Opiates
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Description:
Opioid/Opiates
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  1. Pure opioid agonist
    • morphine
    • codeine
    • activate mu and kappa receptors
  2. mixed agonist-antagonist (partial agonist)
    • nalbuphine (Nubain) 
    • pentazocine (Talwin) 
    • butorphanol (Stadol)
    • buprenorphine (Buprenex)
  3. stages of nociception
    • transduction
    • transmission
    • perception
    • modulation
  4. Meperidine
    • high potency
    • sig. anticholinergic effects
    • seizures with accumulation of metabolite
  5. Fentanyl
    • rapid onset
    • low bioavailability by po
  6. sufentanil (Sufenta)
    5-7x more potent than fentanyl
  7. Remifentanil (Ultiva)
    • metabolism via esterases
    • short duration of action
  8. Methadone
    • treatment of opiate dependence
    • withdrawal has slower onset, more prolonged
    • NMDA antagonist, also blocks MAO reuptake
  9. Diphenoxylate
    • causes constipation
    • atropine added to discourage abuse
  10. Buprenorphine (Buprenex)
    • potent, partial mu receptor agonist
    • resistance to naloxone reversal
  11. Nalbuphine (Nubain)
    • kappa agonist and mu antagonist
    • respiratory depression resistant to naloxone
  12. Butorphanol (Stadol)
    • kappa agonist, partial agonist or antagonist at mu receptor
    • low addictive and abuse liability
  13. Pentazocine (Talwin)
    • kappa agonist, mu partial agonist activity
    • weak antagonistic properties -- precip. a withdrawal attack
  14. Tramadol (Ultram)
    • codeine analog
    • weak mu agonist effects, may also block NE and 5HT reuptake
  15. Naltrexone (ReVia)
    • pure antagonist
    • similar to Narcan

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