Opioids

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Author:
LT24
ID:
32084
Filename:
Opioids
Updated:
2010-08-31 16:02:08
Tags:
Mechanism receptors types
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Description:
Lecture #6
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  1. Types of opioids
    • Naturally occuring
    • Semi-synthetics
    • Synthetics
    • Opioid antagonists
    • Endogenous opioids
  2. Naturally occuring
    • Opium
    • 2 major alkaloids:
    • Morphine
    • Codeine
  3. Semi-synthetics
    • Heroin
    • Analgesics:
    • Hydromorphone - potent
    • Hydrocordone - less potent
    • Oxycodone - strongest
  4. Synthetics
    • Mimic actions of opiates
    • Phenylpiperidines
    • Methadone and congeners
    • Benzomorphans
  5. Opioid antagonists
    • Naloxone - treat heroin overdose
    • Naltrexone
    • Suboxone
  6. Endogenous opioids
    • Enkephalins
    • Endorphins
    • Dynorphins
  7. Analgesic Potency
    • Mild to moderate pain -> codeine, propoxyphene
    • Moderately severe -> meperdine
    • Severe pain -> heroin, hydromorphone
  8. Major effects
    • Analgesia
    • Euphoria
    • Nausea and vomiting
    • Respiratory depression
    • Miosis
    • Gastrointestinal effects
    • Cough suppression
    • Motor effects
  9. Sensitization
    • Psychomotor stimulant effects
    • Rewarding effects
  10. Opioid peptide gene families
    • Proopiomelanocortin (POMC) -> beta-endorphin
    • Proenkephalin
    • Prodynorphin -> dynorphins A and B
  11. Mu receptor
    • Morphine
    • Endorphins
    • Thalamus and caudate
  12. Delta receptor
    • Enkephalins
    • Caudate
  13. Kappa receptor
    • Ketocyclazocine
    • Dynorphin
  14. Mu compound mechanism
    • Increase DA cell firing
    • Increase DA release in nucleus accumbens
    • Locomoter activation
  15. Kappa compound mechanism
    • Decrease DA cell firing
    • Decrease DA release
    • Decrease locomotion
  16. Gastrointestinal effects
    • Mediated by mu and kappa sites
    • In stomach, small and large intestines
    • Decreased motility -> constipation

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