The document discusses opioids, including their definition, sources, receptors, history of use, classifications, mechanisms of action, pharmacological effects, adverse effects, toxicity, and therapeutic uses. It describes the three main opioid receptors (mu, kappa, delta), the effects of receptor activation, and different classifications of opioids based on their receptor actions (agonists, partial agonists, antagonists, mixed). It covers the absorption, distribution, metabolism and excretion of opioids. The major pharmacological actions discussed are analgesia, sedation, respiratory depression, nausea, constipation, and dependence/withdrawal. Therapeutic uses include management of severe pain and obstetrical labor pain. Risks/cautions with impaired organ function and certain patient populations

1. DR.UMA KADAM M.B.B.S. MD ASSOCIATE PROFESSOR PHARMACOLOGY SKNMC

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

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

15. Methylated at C3 Codeine Oxycodone Morphine OH OH

19. Mechanism of action:

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

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