Pharmacology #2 (opioid analgesics)

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Pharmacology #2 (opioid analgesics)
2013-02-19 18:00:52
AA Emory Anesthesia

Drugs and info for Pharm exam 2- opioid analgesics.
Show Answers:

  1. What are the STRONG opioid agonists?
    • Morphine
    • Methadone
  2. What are the moderate opioid agonists?
  3. What are the prototype mixed agonist-antagonist opioids?
    • Pentazocine
    • Buprenorphine
  4. What are the opioid antagonists?
    • Naloxone
    • Naltrexone
  5. What is phasic pain?
    sharp and pricking.  a type of acute pain
  6. what is tonic pain?
    dull, throbbing, aching pain.  a type of acute pain
  7. Define Opiate:
    drug derived from juice of opium poppy (morphine and codeine)
  8. Define Opioid:
    natural or synthetic compounds with actions that mimic morphine
  9. Define Opiopeptin:
    endogenous opioid peptides.   includes endorphins, dynorphins, enkephalins
  10. define Narcotic:
    legal term for these drugs, but not medical term.  derived from greek word for stupor
  11. Mechanism of action (simple):
    interact with endogenous opioid receptors.  Receptors are found mostly in the brain and spinal cord.
  12. what are the 3 types of opioid receptors?
    μ, δ, κ
  13. Mechanism of action of opioid receptors:
    • inhibit voltage-gated Ca channels and decrease the release of NT from presynaptic terminals of nociception afferents.
    • *mu also has post-synaptic action, activing inward K.
  14. μ has high affinity for what?
    • Morphine, enkephalins, B-endophin.
    • endorphins>enk>dyn
  15. μ mediates:
    opioid induced analgesia, + reinforcement, resp depression, miosis, decreased GI motility, neuroendocrine fx
  16. δ receptors have a high affinity for what?
    • enkephalins, and B-endophin.
    • enk>endo and dyn
  17. δ receptors do what?
    antinociception, motor integration, cognitive function
  18. κ receptors have a high affinity for?
    • dyn>> endo/enk
  19. κ receptors do what?
    regulate food intake, temp control, GI motility, pain perception, neuroendocrine fx
  20. where are opioid receptors found?
    • primary afferents and spinal cord pain transmission neurons.
    • also descending pain pathways- PAG and RVM
    • brain stem, hypothalmus, GI tract
  21. Mechanism of opioids
    • inhibit release of excitatory response NT's.
    • acitivate pain inhibitory pathways form spinal cord
  22. Opioid fx on CNS:
    • analgesia
    • eu or dysphoria
    • sedation
    • resp depression
    • cough suppression
    • Miosis (pupil constriction)
    • Emesis
  23. Opioid fx on CV system:
    hypotension and vasodilation
  24. Opioid fx on GI system:
  25. Opioid fx on GU system:
    urinary retention, prolonged labor
  26. Opioid fx on neuroendocrine system:
    stimulates release of ADH and prolactin. inhibits leutenizing hormone
  27. Opioid fx on dermis:
    flushing, itching, urticaria
  28. Tolerance to most fx except:
    constipation, miosis
  29. Can cross-tolerance occur?
  30. Withdrawal syndrome:
    lacrimation, rhinorhea, yawn, chills, hypervemitlation, muscle spasms, vomiting, anxiety and hostility
  31. what are strong agonists used to treat? ehat drugs are in this category?
    • severe pain. 
    • morphine,heroin, methadone, meperidine, fentanyl
  32. strong agonists have a strong affinity for which receptor?
  33. Facts about morphine:
    • active ingredient in OPIUM
    • 4-6 hr duration
    • has active metabolite: morphine-6-glucuronide
    • TX of sever pain
  34. Methadone facts:
    • LONG duration- 15-20 hrs
    • orally effective
    • used for detox and withdrawal
  35. what drug is used to treat withdrawal of morphine and heroin?
  36. Fentanyl facts:
    • 80x potent than morphine
    • rapid onset, short duration
    • used as an anesthesia adjunct
  37. Name a moderate antagonist:
  38. Codeine facts:
    • 0.5% of opium
    • not active until metabolized to morphine
    • given for mild to moderate pain in combo with aspirin and tylenol
    • included in many cough syrups
  39. Moderate agonists are used for _______ and and have  potential for _______.  They are usually _______ with other non-opioid analgesics.
    moderate pain tx, abuse, mixed
  40. Mixed agonist-antagonists:
    have agonist fx on one receptor type, antagonist on others
  41. What are the Mixed agonist-antagonists:
    • pentazocine
    • buprenorphine
  42. pentazocine facts:
    • k-agonist, weak mu antagonist
    • parenteral formula used as preanesthetic
    • orally for moderate to severe pain
    • precipitates a withdrawal syndrome in morphine abuser
  43. Buprenorphine facts:
    • potent, long lasting partial mu-agonist
    • slow dissociation from mu-receptor makes it resistant to naloxone
    • effective tx for cocaine and heroin abusers
  44. What are the opioid antagonists?
    naloxone and naltrexone
  45. naloxone facts:
    • competitive antagonist at mu>delta=k
    • 1-2 hr duration
    • no fx on normal individuals
    • will cause withdrawal in opiate abusers
    • IV use to reverse opioid overdose
  46. naltrexone:
    • long lasting competitive antagonist (24hrs)
    • used as maintenance drug for addicts
    • tx of alcohol craving
  47. what drug is used to treat alcohol craving in chronic alcoholics?
  48. what drug is resistant to naloxone reversal?
  49. what drugs will cause withdrawal syndrome in opioid abuser?
    pentazocine, naloxone
  50. what is the active metabolite of morphine?