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Opioid analgesics
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Opioid analgesics

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  • 1. Opioid Analgesics
  • 2.
    • Strong
    • Morphine
    • Methadone
    • Meperidine
    • Moderate
    • Codeine
    • Oxycodone
    • Weak
    • Propoxyphene
    • Mixed (agonists- antagonists)
    • Buprenorphine, nalbuphine
  • 3.
    • Antagonists
    • Naloxone
    • Naltrexone
  • 4. Clinical Uses
    • Analgesia- Fentanyl, morphine
    • Cough Supression- Codeine, Dextromethorphan.
    • Antidiarrheal- Diphenoxylate, Loperamide
    • Acute Pulmonary edema- Morphine
    • Anesthesia- Fentanyl
    • Opioid Dependence- Methadone
  • 5. Pharmacokinetis
    • Well absorbed orally
    • Morphine, hydromorphone, oxymorpine undergo first-pass metabolism.
    • Cross placental barrier and effect fetus, cause respiratory depression, physical dependence in neonates.
    • Metabolism: by hepatic enzymes, inactivated by glucuronide conjugates before elimination from kidneys.
    • Morphine -6- glucuronide (analgesic)
    • Morphine-3- glucuronide ( neuroexcitatory)
  • 6. Mechanism of action
    • Opioids produce analgesia by binding to specific G protein coupled receptors in brain & spinal cord
  • 7. Mechanism of action
    • Receptors
    • μ , δ , κ receptors.
    • All 3 subtypes are involved in antinociceptive and analgesic mechanisms at both spinal and supraspinal levels.
    • μ receptors -respiratory depressant+ GI
    • δ receptors- development of tolerance
    • κ receptors- involved in sedation + GI
  • 8.  
  • 9.
    • Opioid peptides
    • β -endorphin, ( μ ,receptors)
    • Enkephalins ( δ receptors )
    • Dynorphins ( κ receptors)
    • Modulate transmission in brain, spinal cord, adrenal medulla and neural plexus of gut.
  • 10.
    • All 3 receptors are in high concentration in dorsal horn of spinal cord.
    • Direct application of opioid agonists at spinal cord produce regional analgesia.
    • Resp. depression, nausea, vomiting, sedation from supraspinal action.
  • 11. Ionic Mechanisms
    • Presynaptic level close voltage gated Ca+ channels, and reduce transmission.
    • Post synpatic level open K+ channels (inhibit post synaptic neurons).
  • 12.  
  • 13. EFFECTS
    • Analgesia
    • Most powerful analgesics,
    • Morphine, methadone, meperidine, fentanyl, heroin
    • Sedation and euphoria
    • Respiratory depression
    • Action at medulla lead to respiratory depression .
    • Antitussive effects
    • Suppression of the cough reflex
    • Nausea & vomiting
    • Activation of chemoreceptor trigger zone
  • 14. Side Effects
    • GI effects
    • Constipation with decreased intestinal peristalsis.
    • Smoot muscle
    • Cause contraction of billiary billiary tract SM, inc. ureter and bladder tone, red. Uterine tone (prolong labor)
    • Miosis
    • Tolerence
    • Dependence
  • 15. Toxicity
  • 16. Treatment of Opioid Poisioning
  • 17.  

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