Opioids

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Author:
xinchen3
ID:
195703
Filename:
Opioids
Updated:
2013-01-27 13:11:14
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Opioids
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Description:
Opioids
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  1. What are the Endogenous Opioids and their targets receptors?
    • Endorphins - mu receptors
    • Enkephalins - delta receptors
    • Dynorphins - kappa receptors
  2. Opioid MoA
    • - inhibits neurotransmission at synapse
    • - decrease presynaptic release
    • - decrease postsynaptic excitability
    • - decrease substance P release at Spinal Cord
  3. Opioid - Uses
    • - severe pain managements
    • - cancer, labor (cross placenta, can cause flaccid baby syndrome)
  4. Opioids - Adverse Effects
    • sedation
    • constipation
    • respiratory depression/muscle suppression
    • nausea & vomiting
    • addiction/abuse/dependence/tolerance
  5. Morphine
    • mu receptors agonist
    • Pros:
    • no ceiling effects
    • patient-controlled analgesia
    • Use:
    • Adjunct in anesthesia
    • pulmonary edema
  6. Methadone
    • mu receptor agonist
    • NMDA antagonist
    • monoamine reuptake inhibitor
    • Use:
    • rehabilitation of other drugs
    • Cons:
    • prolong QT interval & arrhthymia
  7. Fentanyl
    (Sufentanyl, Alfentanyl, Remifentanyl)
    • mu receptor agonist
    • Use:
    • adjunct in anesthesia
  8. Hydromorphone, Oxymorphone
    • mu receptor agonist
    • more potent than morphine
  9. Meperidine
    • mu receptor agonist
    • has anti-cholinergic effects
  10. Oxycodone
    • mu receptor agonist
    • has ceiling effect, dose dependent
  11. Codeine
    • mu receptor agonist
    • less potent than morphine, but converts to morphine in body by CYP2D6
    • (there is a genetic defect in caucasians that lack this enzyme, Codeine doesn't work)
  12. Dextromethorphan
    • mu receptor agonist
    • NO analgesic effects and addictive potentials
    • less constipations
    • Use: Anti-tussive (cough medications)
  13. Nalbuphine
    Nalorphine
    Levallorphan
    • k agonist, mu antagonist
    • has ceiling effect
  14. Buprenorphine
    • k agonist, mu antagonist
    • Use: rehabilitation programs (alternative to Methadone)
    • Cons: hallucination, nightmare & anxiety when used with Pentazocine & Nalbuphine
  15. Tramadol
    Tapentadol
    • mu-partial agonist
    • block 5-HT & NE reuptake (prolong effects)
    • Cons
    • Seizure (prolonged NE, avoid MAO inhibitors)
    • Serotonine syndrome (prolong 5-HT)
  16. Naloxone (short acting)
    Naltrexone (long acting)
    Nalmefene (IV only)
    Methylnaltrexone
    • opioid ANTAGONIST
    • Uses:
    • Opioid overdose
    • alcohol & opioid dependence
    • opioid-induced constipation

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