Pharm Test 4: Opioids

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BrookeNH10
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201340
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Pharm Test 4: Opioids
Updated:
2013-02-17 23:50:04
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Pharm Test Opioids
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Pharm Test 4 Opiods
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  1. Opioids vs. Opiates vs. Endogenous opioids
    • Opioids= all-encompassing term
    • Opiates= Alkaloid pharmaceuticals (morphine, codine)
    • Endogenous Opioids= Peptides (precursor proteins)
  2. Origin of opiates
    Seed of opium poppies
  3. Rank in order of strength:  Morphine, Codeine, Thebaine
    Morphine > Codeine > Thebaine
  4. Morphine is the parent molecule.  When you add a -CH3 you get
    Codeine
  5. Morphine is the parent compound.  When you add 2 acetyl (CH3OO)2 what do you get?
    Heroin
  6. 4 Therapeutic Categories of Opioids
    • Strong Agonists (morphine)
    • Mild/Moderate Agonists (codeine)
    • Mixed Agonists/Antagonists (Buprenorphine, Butorphanol, Pentazocine)
    • Narcotic Antagonists (Naloxone, Alvimopam)
  7. Receptor that mediates opioid's analgesic and euphoric effects
    Mu opioid receptor
  8. Receptor that mediates opioid's sedation and dysphoric effects
    Kappa opioid receptor
  9. Epsilon receptor is preferentially selective for
    B-endorphin
  10. Opioid receptors= what type of receptor
    G-coupled receptor
  11. 5 Clinical Uses of Opioids
    • Analgesia
    • Acute Pulmonary Edema
    • Cough
    • Diarrhea
    • Adjuncts to anesthesia
  12. 3 Side effects of Opioids
    • Miosis
    • Constipation
    • Increased intracranial pressure
  13. 2 side effects of opioids that are resistant to tolerance
    • Miosis
    • Constipation
  14. 4 CNS Effects of Opioids
    • Truncal rigidity
    • Respiratory depression
    • Miosis (Edinger-Westphal Nucleus)
    • Inhibits sexual drive (w/ repeptitive use)
  15. Opioids MoA:
    Presynaptic Neurons
    Kappa, Delta, and Mu receptors present

    • Decreases calcium influx
    • Decreases transmitter release
  16. Opioids MoA:  Postsynaptic Neurons
    Increases K+ conductance -> IPSP
  17. 4 Sites of Opioid Action
    • 1)Block Afferent Pain:  Substantia gelatinosum @ dorsal horn of spinal cord
    • 2)Activate descending inhibitory pain pathway in brain that descends to spinal cord
    • 3)Relieve emotional pain by acting on thalamic nuclei
    • 4)Mediate pain of inflammation by acting on peripheral receptors
  18. 4 Sites of Opioid Action
    • Dorsal horn (spinal cord)
    • Midbrain
    • Medulla
    • Thalamic Nuclei
  19. 3 Strong Agonists
    • Morphine
    • Methadone
    • Meperidine
  20. Can opioids be administered orally?
    Oral route is less effective due to significant hepatic first-pass metabolism
  21. Opioid Pharmacokinetic Distribution
    • Lipid soluble (for CNS penetration); Heroin, codeine, methadone > morphine
    • Concentrate in tissue (skeletal muscle primary reservoir)
    • Readily crosses placenta
  22. Major active hepatic metabolite of Morphine
    Morphine-6B-glucuronide
  23. Primary alkaloid in opium
    Morphine
  24. 10x more potent than morphine, high abuse liability (no longer used in US)
    Hydromorphone
  25. Another name for heroin
    Diacetylmorphine (Schedule I)
  26. Lollipopo or transdermal patch
    Fentanyl
  27. Tends to dilate pupils
    Meperidine
  28. 2 things Meperidine is NOT used for
    Cough, diarrhea
  29. Causes tremors, convulsions w/ large doses
    Meperidine
  30. Meperidine + MAOIs=
    Hyperpyrexic coma
  31. Can cause serotonin syndrome
    Meperidine
  32. Opioid tolerance
    Incomplete cross-tolerance (use an opiod rotation)
  33. Single crushed 80mg tablet is lethal in naive user
    Oxycodone
  34. Antitussive effects
    Codeine
  35. 2 Mild Opioid Agonists used to treat diarrhea
    • Diphenoxylate
    • Loperamide (Imodium)
  36. Active at more than one opioid receptor, but may block analgesic actions of pure agonists
    Mixed Agonists/ Antagonists (Buprenorphine, Butophanol, Pntazocine, Dezocine)
  37. Weak MOP agonist, blocks NE and 5HT uptake in CNS (Analgesic action not entirely opioid dependent)
    Tramadol
  38. Seizures, suicide risk
    Tramadol
  39. Selective antitussive w/ no analgesia
    Dextromethorphan
  40. Dextromethorphan is an antagonist at what receptor
    NMDA glutamate receptors
  41. Narcotic antagonist that can show acute elevation in BP
    Naloxone
  42. Opioid withdrawal symptoms?  Tx?
    Nausea, vomiting, rhinorrhea

    Naloxone
  43. Narcotic Antagonists that restore bowel function
    • Alvimopan
    • Methylnaltexone bromide
  44. Do NOT use opioids in labor or head trauma!
  45. Triad of acute opioid intoxication
    • Coma
    • Pinpoint pupils
    • Depressed respiration

    Tx:  Naloxone
  46. Most abused opioids are
    Prescribed
  47. Narcotic used for long-term pain that caused seizure
    Meperidine
  48. Dextromethrophan is most likely to have been administered for
    coughing relief
  49. Associated w/ confusion and seizures
    Normeperidine
  50. Recovering from abdominal surgery, presents w/ pinpoint pupils and constipation.  Most likely taking
    Hydromorphone (dilauded)
  51. Manage opioid addicts
    Methadone
  52. Exhibits the greates propensity for euprhoria and abuse liability
    Hydromorphone (dilauded)
  53. Exerts its actions solely in the periphery rather than in the CNS
    Alvimopan
  54. Manage long-term opioid withdrawal with
    Promethazine (Phenergan) and Clonidine

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