pain and opioid pharm

  1. morphine
    • MOA: full mu agonist, high analgesic effect
    • USES: moderate to severe pain assciated with cancer, MI, relief of dyspnea
    • purified from opium
    • AE: resp depression, , N/V, increased ICP, urinary retention
  2. methadone
    • MOA: full mu agonist, MAOI, NMDA receptor antagonist
    • USES: opioid abuse, useful in opioid rotation - due to when a tolerance develops, can become hypersensitive to pain
    • AE: prolonged QT interval, cardia arrhythmia
    • decrease metabolism, increase risk of resp depression
  3. meperidine
    • MOA: mu receptor full agonist, antimuscarinic
    • USES: no longer first line analgesic due to AE profile
    • AE: tachycardia, seizures
  4. fentanyl
    • MOA: Mu receptor full agonist, strong
    • USES: most used synthetic opioids, relief of moderate to severe pain, post operative or labor analgesia, chronic pain (transdermal patch), breakthrough pain in cancer (buccal tablet, lollipop)
    • AE: no histamine release - no puritis, chest muscle rigidity of infused IV too quickly
    • short onset of action
  5. codeine
    • MOA: mu receptor full agonist, moderate
    • USES: relief of mild to moderate pain, antitussive in selected pts. 
    • partly biotransformed to morphine - likely responsible for its analgesic effects
  6. tramadol
    • MOA: inhibition of NE and serotonin reuptake, mu receptor full agonist, analgesic effect is only partially inhibited by naloxone
    • USES: relief of mild to moderate pain, chronic neuropathic pain
    • AE: less constipation, less resp depression, then morphine precipitation of withdrawl on abrupt discontinuation
    • synthetic codeine analogue,
    • CI: pts with a history of opioid abuse/addiction
  7. pentazocine
    • MOA: Mu receptor partial agonist
    • USES: relief of moderate to severe pain, preoperative sedative and as a supplement to anesthesia
    • AE: tachycardia, HTN
  8. buprenorphine
    • MOA: mu receptor partial agonist, Kappa and delta antagonists, slow dissociation from mu receptors
    • USES: relief of moderate to severe acute-MI or chronic-transdermal patch, opioid dependence
  9. naloxone
    • MOA: opioid antagonist
    • USES: acute opioid overdose (short DOA must be taken into account)
    • AE: precipitete withdrawl syndrome
    • all rapid routes of admin that avoid first pass, rapid onset
    • CI: crosses placenta
  10. naltrexone
    • MOA: opioid antagonist
    • USES: ethanol dependence, maintenance tx to prevent release in opioid dependent pts
    • AE: injection site rxn
    • longer duration of action than naloxone
    • CI: narcotic dependent or current use of opioid analgesic, compromised liver function
Card Set
pain and opioid pharm
pain and opioid pharm