pharm II test II opiods

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pharm II test II opiods
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pharm II test II opiods
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  1. 2 opioid agonists
    • morphine - strong
    • codeine - moderate
  2. 3 mixed opioid agonist/antagonist (partial agonists)
    • pentazocine - Talwin
    • butorphanol
    • buprenorphin - buprenex
  3. pure opioid antagonist
    naloxone -
  4. 2 endogenous ligands for Mu receptor
    • enkephalins
    • beta endorphins
  5. endogenous ligand for Kappa receptor
    dynorphins
  6. 2 endogenous ligands for delta receptor
    • enkephalins
    • beta endorphin
  7. 5 drug ligands for Mu receptors
    • morphine
    • fentanyl
    • methadone
    • meperidine
    • buprenorphine
  8. 2 drug ligands for Kappa receptors
    • pentazocine
    • butorphanol
  9. 3 drug ligands for Delta receptors
    • sufentanil
    • morphine
    • codeine
  10. 4 clinical effects of the Mu receptor
    • analgesia
    • euphoria
    • respiratory depression
    • physical dependence
  11. 3 clinical effects of the Kappa receptor
    • analgesia at the spinal cord level
    • sedation
    • dysphoria
  12. clinical effects of Delta receptors
    may contribute to anagesia
  13. 3 mechanisms on the opiate receptors
    • coupled to adenylyl cyclase through Gi, decreases cAMP
    • decrease Ca2+ conductance on presynaptic terminals = decrease release of neurotransmitters
    • increased K+ conductance on postsynaptic neurons = hyperpolarization and inhibition
  14. the most lipophilic opioid
    fentanyl
  15. what makes fentanyl short action even though it has a longer half life than morphine
    rapid redistribution in the tissues; liver, spleen, kidney and lung
  16. morphine metabolism
    • conjugated to
    • morphine-3-glucuronide M3G - inactive but has neuroexcitatory effects
    • morphine-6-glucuuronide M6G - more potent than morphine but slowly crosses the BBB
  17. heroin metabolism
    • hydrolyzed to
    • 6-mono-acetylmorphine - active
    • morphine
  18. codeine metabolism
    • CYP2D6
    • 10% O-demethylated to morphine
  19. meperidine metabolism
    • N-demethylation to
    • normeperidine - can cause seizures if it accumulates especially in children
  20. fentanyls metabolism
    CYP3A4 intestinally - dealkylation
  21. pharmacological action of morphine in analgesia
    Reduces the affective response to pain stimulation and increases pain tolerance without altering the threshold for perception of the stimulus.
  22. pharmacological action of morphine on respiratory depression
    Decreased responsiveness to increases in CO2 concentration; also depresses centers involved in regulating rhythmicity.
  23. pharmacological action of morphine on the GI tract
    Delays passage of GI contents due to increase in tone and sphincter spasm.
  24. pharmacological action of morphine on cardiovascular system
    • postural hypotension
    • vasodilation
    • CO2 retention and increase in CSF pressure
  25. meperidine
    • phenylpiperidine
    • CNS effects comparable to morphine but shorter acting & less effect on smooth muscle.
    • Significant anticholinergic effects
    • Seizures with accumulation of metabolite, normeperidine.
    • Contraindicated with MAOI
  26. Remifentanil - ultiva
    • phenylpiperidine
    • approved for surgical analgesia; metabolized very rapidly by plasma esterases → very short duration of action (3-4)minutes
  27. Sulfentanil - sulfenta
    • phenylpiperidine
    • 5-7 times more potent than fentanyl.
  28. fentanyl
    • phenylpiperidine
    • Rapid onset and short duration; used in anesthesiology
  29. methadone
    • phenylheptylamine
    • pharmacological properties qualitatively similar to morphine
    • longer duration of action
    • more effective orally
    • withdrawal has a slower onset, more prolonged
  30. levomethadyl - orlaam
    • phenylheptylamine
    • approved for use in detoxification clinics; may be given once every 2-3 days.
  31. codeine
    • phenanthrene
    • lower analgesic potency 
    • lower addiction liability than morphine
    • very high oral efficacy
    • antitussive
    • Usually combined in formulations containing aspirin, acetaminophen or other drugs for analgesia*.
  32. diphenoxylate - lomotil
    • phenylpiperidine
    • prominent effect is constipation
    • atropine added primarily to discourage abuse
  33. loperamide - imodium
    • phenylpiperidine
    • anti-diarrheal 
    • potential for abuse is low because very little crosses BBB
  34. buprenorphine - subutex
    • phenanthrene
    • long acting Mu receptor agonist
    • parenterally for sever pain
    • slow dissociation causing long duration and resistance to naloxone
  35. nalbuphine - nubain
    • phenanthrenes
    • kappa agonist
    • Mu antagonist
    • ceiling to respiratory depression but resistant to naloxone
  36. butorphanol - stadol
    • morpinan
    • predominantly Kappa agonist
    • parenterally produces analgesia =to bupronex
  37. pentazocine - talwin
    • predominantly Kappa
    • moderate analgesic weak antagonistic
  38. tramadol - ultram
    • analog of codeine
    • weak Mu agonist
    • analgesic effect from block of NE 5HT reuptake (mainly 5HT)
  39. tapentadol - nucynta
    • more potent version of tramadol
    • more effect on decreasing NE reuptake
  40. dextromethorphan
    • non-narcotic
    • no analgesia or addictive properties
    • anti-tussive
  41. naloxone - narcan
    • opioid antagonist
    • duration 1-2 hrs
    • highest affinity for Mu receptors
    • few effects when given w/o agonist
    • reversal in 1-3 min. of IV administration
    • no tolerance
  42. naltrexone - ReVia
    • opioid antagonist
    • duration 48 hrs
    • oral
  43. nalmefene - Revex
    • opioid antagonist
    • IV
    • duration 8-10 hrs
  44. methylnaltrexone - relistor
    • peripheral antagoinist
    • Tx of constipation

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