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Opioid analgesics
 

Opioid analgesics

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    Opioid analgesics Opioid analgesics Presentation Transcript

    • Opioid Analgesics
      • Strong
      • Morphine
      • Methadone
      • Meperidine
      • Moderate
      • Codeine
      • Oxycodone
      • Weak
      • Propoxyphene
      • Mixed (agonists- antagonists)
      • Buprenorphine, nalbuphine
      • Antagonists
      • Naloxone
      • Naltrexone
    • Clinical Uses
      • Analgesia- Fentanyl, morphine
      • Cough Supression- Codeine, Dextromethorphan.
      • Antidiarrheal- Diphenoxylate, Loperamide
      • Acute Pulmonary edema- Morphine
      • Anesthesia- Fentanyl
      • Opioid Dependence- Methadone
    • 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)
    • Mechanism of action
      • Opioids produce analgesia by binding to specific G protein coupled receptors in brain & spinal cord
    • 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
    •  
      • 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.
      • 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.
    • Ionic Mechanisms
      • Presynaptic level close voltage gated Ca+ channels, and reduce transmission.
      • Post synpatic level open K+ channels (inhibit post synaptic neurons).
    •  
    • 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
    • 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
    • Toxicity
    • Treatment of Opioid Poisioning
    •