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DR.UMA KADAM   M.B.B.S. MD ASSOCIATE PROFESSOR PHARMACOLOGY SKNMC
[object Object],Opioids: Narcotic:  imprecise term suggesting "narcosis": indicated of a somnolent state  Opioid analgesic:  analgesia (pain absence) without resulting in loss of consciousness/sleep Opioids:  Definition all natural/ semisynthetic opium alkaloid derivatives  synthetic agents other drugs whose opioid-like effects  are blocked by naloxone -nonselective opioid receptor antagonist  Source:   Opium from the opium poppy Constituents:  morphine  codeine  Thebaine : nonanalgesic  Papaverine -- nonanalgesic, vasodilator
Opioids ,[object Object],[object Object],[object Object],[object Object],[object Object]
History of Opioids ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Natural opioids occur in 2 places: ,[object Object],[object Object],[object Object]
Three Opioid Receptors ,[object Object],[object Object],[object Object]
Mu-Receptor: Two Types ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Kappa Receptor ,[object Object],[object Object],[object Object],[object Object]
Delta Receptor ,[object Object],[object Object],[object Object]
No effect Decrease contraction δ Mouse vas deferens No effect Decrease contraction u Guinea pig ileum       Isolated organ bioassays   Inhibit u, δ Dopamine   Inhibit u Acetylcholine       Neurotransmitter release Decrease release Increase release u and/or δ Growth hormone Decrease release Increase release u Prolactin       Hormone regulation   Increase κ Diuresis No effect Increase u, κ Sedation Decrease feeding Increase feeding u, κ, δ Feeding No effect Increase κ Psychotomimesis No effect Decrease transit u, κ Gastrointestinal tract No effect Decrease u Respiratory function No effect Analgesic u, κ, δ Spinal No effect Analgesic u, κ, δ Supraspinal       Analgesia Antagonist Agonist RECEPTOR SUBTYPE      
Mu and Kappa Receptor Activation Physical Dependence Decrease GI motility Dysphoria Euphoria Respiratory Depression Analgesia Kappa Mu-2 Mu-1 Response
Terminology ,[object Object],[object Object],[object Object],[object Object]
Classification of Opioids: Agonist Partial Agonist/weak antagonist Partial Agonists Pentazocine Antagonist Antagonist Pure Antagonists Naloxone, Naltrexone Agonist Antagonist Agonist-Antagonist  Nalbuphine, butorphanol, Buprenorphine  Agonist Agonist Pure Agonists   Morphine, codeine, meperidine,  fentanyl , remifentanil, propoxyphene , hydrocodone , oxycodone  KAPPA MU DRUGS
Chemical substitutions: ,[object Object],[object Object],[object Object],[object Object],[object Object]
Methylated at C3 Codeine Oxycodone Morphine  OH OH
Pharmacokinetics: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Pharmacokinetics: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Mechanism of action ,[object Object],[object Object],Spinal Cord Sites of Opioid Action K+ Ca++
Mechanism of action:
Mechanism of action: ,[object Object]
Pharmacological actions: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Pharmacological actions: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Pharmacological actions: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],Pharmacological actions:
Pharmacological actions: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Pharmacological actions: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Pharmacological actions: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],Pharmacological actions:
Pharmacological actions: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Adverse effects: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Opioid Effects: Degree of Tolerance Developed       Convulsions    Mental  clouding Constipation    Euphoria, dysphoria Miosis Bradycardia  Analgesia  Limited/None Intermediate High   Cough  suppression   Nausea / vomiting   Antidiuresis   Respiratory depression Antagonist actions   Sedation
Some Symptoms of Opioid Withdrawal Hyper ventilation Yawning Piloerection Hostility Diarrhea Anxiety Vomiting Muscular aches Hyper ventilation Chills Lacrimation Rhinorrhea
[object Object],[object Object],[object Object],[object Object],Adverse effects:
Treatment: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Contraindications/Therapeutic Cautions:   ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Therapeutic uses: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Therapeutic uses: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Methadone (Phenylheptylamines) ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Phenylpiperidines (e.g. Meperidine, fentanyl, Diphenoxylate, Loperamide)  ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
Opioid agonist-antagonists: ,[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object],[object Object]
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Opioids

  • 1. DR.UMA KADAM M.B.B.S. MD ASSOCIATE PROFESSOR PHARMACOLOGY SKNMC
  • 2.
  • 3.
  • 4.
  • 5.
  • 6.
  • 7.
  • 8.
  • 9.
  • 10. No effect Decrease contraction δ Mouse vas deferens No effect Decrease contraction u Guinea pig ileum       Isolated organ bioassays   Inhibit u, δ Dopamine   Inhibit u Acetylcholine       Neurotransmitter release Decrease release Increase release u and/or δ Growth hormone Decrease release Increase release u Prolactin       Hormone regulation   Increase κ Diuresis No effect Increase u, κ Sedation Decrease feeding Increase feeding u, κ, δ Feeding No effect Increase κ Psychotomimesis No effect Decrease transit u, κ Gastrointestinal tract No effect Decrease u Respiratory function No effect Analgesic u, κ, δ Spinal No effect Analgesic u, κ, δ Supraspinal       Analgesia Antagonist Agonist RECEPTOR SUBTYPE      
  • 11. Mu and Kappa Receptor Activation Physical Dependence Decrease GI motility Dysphoria Euphoria Respiratory Depression Analgesia Kappa Mu-2 Mu-1 Response
  • 12.
  • 13. Classification of Opioids: Agonist Partial Agonist/weak antagonist Partial Agonists Pentazocine Antagonist Antagonist Pure Antagonists Naloxone, Naltrexone Agonist Antagonist Agonist-Antagonist Nalbuphine, butorphanol, Buprenorphine Agonist Agonist Pure Agonists Morphine, codeine, meperidine, fentanyl , remifentanil, propoxyphene , hydrocodone , oxycodone KAPPA MU DRUGS
  • 14.
  • 15. Methylated at C3 Codeine Oxycodone Morphine OH OH
  • 16.
  • 17.
  • 18.
  • 20.
  • 21.
  • 22.
  • 23.
  • 24.
  • 25.
  • 26.
  • 27.
  • 28.
  • 29.
  • 30.
  • 31. Opioid Effects: Degree of Tolerance Developed       Convulsions   Mental clouding Constipation   Euphoria, dysphoria Miosis Bradycardia Analgesia Limited/None Intermediate High   Cough suppression   Nausea / vomiting   Antidiuresis   Respiratory depression Antagonist actions   Sedation
  • 32. Some Symptoms of Opioid Withdrawal Hyper ventilation Yawning Piloerection Hostility Diarrhea Anxiety Vomiting Muscular aches Hyper ventilation Chills Lacrimation Rhinorrhea
  • 33.
  • 34.
  • 35.
  • 36.
  • 37.
  • 38.
  • 39.
  • 40.