med chem III quiz 4 analgesics

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med chem III quiz 4 analgesics
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med chem III quiz 4 analgesics
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  1. receptor responsible for analgesia, euphoria, respiratory depression and physical dependence
    Mu
  2. receptor responsible for mixed-action agonists and analgesia at the level of the spinal cord, sedation and dysphoria
    Kappa
  3. receptor may contribute to analgesia
    Delta
  4. 6 Mu ligands
    • endorphins
    • enkephalins
    • morphine
    • fentanyl
    • methadone
    • meperidiine
  5. 3 Kappa ligands
    • dynorphins
    • pentazocine
    • butorphanol
  6. 4 delta ligands
    • enkephalins
    • endorphins
    • morphine
    • codiene
  7. Kappa receptor mechanism
    decreased Ca2+ conductance
  8. MU receptor mechanism
    increased K+ conductance
  9. delta receptor mechanism
    increased K+ conductance
  10. natural phenanthrene
    full Mu receptor agonist
    ind - analgesic activity and preoperative anesthetic agent
    morphine - avinza
  11. natural phenanthrene
    partial agonist of the Mu receptor
    effective anti-tussive less analgesic
    codeine
  12. opium tincture
    used to treat diarrhea and as an analgesic
    codeine
  13. semi-synthetic phenanthrene
    full agonist at the Mu receptor
    less analgesic and respiratory depression than morphine
    used alone for anti-tussive effects
    hydrocodone - lortab
  14. semi-synthetic phenanthrene
    full agonist at the Mu receptor
    equipotent to morphine
    oxycodone
  15. controlled release oxycodone
    oxycontin
  16. immediate release oxycodone
    oxecta
  17. combo oxycodone and APAP
    roxicet
  18. combo oxycodone and ASA
    percodan
  19. semi-synthetic phenanthrene
    full agonist at the Mu receptor
    equipotent analgesic and respiratory depression but less constipation
    hydromorphone
  20. extended release hydromorphone
    exalgo
  21. hydromorphone tablet, liquid or injection
    dilaudid
  22. semi-synthetic phenanthrene
    full agonist at the Mu receptor
    10X as potent as morphine IV
    weakest anti-tussive agent
    most potent respiratory depression and intense physical dependence of all agents
    don't us in pts < 18 yo or hepatic failure
    oxymorphone
  23. injection oxymorphone
    opana
  24. synthetic phenylpiperidine
    ind - support of anesthesia and obstetrical analgesia
    less smooth muscle spasms, constipation and depression of the cough reflex
    oral and parenteral
    meperidine - demerol
  25. synthetic phenylpiperidine
    very potent agent
    ind - analgesic adjunct in intubated and ventilated patients, major CV or neuro-surgery anesthesia
    sufentanil - sufenta
  26. synthetic phenylpiperidine
    adjunct analgesia in incremental dosing
    dose individualized not for < 12yo
    alfentanil - alfenta
  27. synthetic phenylpiperidine
    very dangerous due to respiratory depression due to high lipid solubility
    fentanyl
  28. synthetic phenylpiperidine
    extremely potent analgesic agent
    ind - induction of anesthesia
    watch for interuption during infusion
    do no administer into same IV line as blood products
    remifentanil - ultiva
  29. synthetic diphenylheptane
    ind - detoxification and maintenance of narcotic addiction (heroin)
    methadone - dolophine, methadose
  30. opiate agonist/antagonist
    ind - mediate morphine like analgesia, euphoria and respiratory and physical depression
    buprenorphine - buprenex
  31. partial opiate agonist
    equipotent to naloxone
    buprenorphiine - buprenex
  32. opiate agonist/antagonist
    transdermal product
    buprenorphine - butrans
  33. pure opiate antagonist
    ind - narcotic overdose
    very short duration of action
    possible use in alcoholism
    naloxone - narcan
  34. what gives opiate a pure antagonist action
    N-allyl substituition
  35. opiate agonist/antagonist
    first analgesic dosage form approved that can be prescribed in a doctor's office
    buprenorphine & naloxone - suboxone
  36. opiate agonist/antagonist
    opiate
    ind - nasal spray --> migraines
           injection --> pain management
    1/40th activity of naloxone
    moa - K agonist, 5X potentcy of morphine
    butorphanol tartrate - stadol
  37. opiate agonist/antagonist
    opiate
    2nd weakest antagonist
    nalbuphine
  38. opiate agonist/antagonist
    opioid
    injection and oral
    heroin substitute w/ tripelennamine
    pentazocine lactate - talwin
  39. non-schedule agent with narcotic agonistic activity
    opioid
    moa - binds Mu and prevents NE and 5HT reuptake in the CNS
    modify dose for CrCl < 30
    metabolized by CYP2D6
    tramadol - ultram
  40. centeral analgesic
    moa - alpha 2 agonist
    oral, or epidual for analgesic
    clonidine - duraclon
  41. ER tab central analgesic foe ADHD
    clonidine - Kapvay
  42. Central analgesic agent
    moa - Mu agonist
             inhibit NE reuptake
    tablet 18X less potent as morphine
    tapentadol - nucynta
  43. central analgesic agent
    antipyretic - inhibits heat regulating center
    pain - inhibits prostaglandin synthase in the CNS mainly
    acetaminophen
  44. IV APAP
    ofirmev
  45. used to treat APAP overdose
    N-Acetylcysteine
  46. conopeptides or conotoxin
    derived form snail
    moa - binds to N type Ca2+ (A-delta and C)
    induces decreased GI motility but not respiratory depression
    CI in psychosis pts
    zirconitide - prialt
  47. CNS agent for pain relief
    ind - postherpetic neuralgia pain
    first drug approved for fibromyalgia
    binds to alpha2-delta site
    structural analog of GABA
    pregabalin - lyrica
  48. pain relief agent
    ind - post herpetic neuralgia
    moa - binds to VR1
    capsaicin - qutenza

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