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Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
Opioids
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Opioids

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  • 1. Opioids (Narcotics) “ Among the remedies which it has pleased Almighty God to give to man to relieve his sufferings, none is so universal and so efficacious as opium.”
  • 2.  
  • 3.  
  • 4. Ancient History <ul><li>Opium </li></ul><ul><ul><li>The sap of the seed pod of Papaver somniferum, referred to as early as 3000 BC. </li></ul></ul><ul><ul><li>Found in Spanish burial sites c.4200 BC </li></ul></ul><ul><li>Greeks/Romans </li></ul><ul><ul><li>Used to produce constipation, sleep, panacea </li></ul></ul><ul><ul><li>God Morpheus (God of Dreams) </li></ul></ul>
  • 5. &nbsp;
  • 6. Recent History
  • 7. &nbsp;
  • 8. &nbsp;
  • 9. Opioids (God Morpheus of Dreams) Narcotics (Narcosis—stupor) <ul><li>Produce analgesia by binding to opiate receptors in the CNS, brain and spinal cord involved with the transmission of pain impulses. </li></ul><ul><li>Produce Morphine like effects on the opioid receptors </li></ul>
  • 10. Pain Neuro Transmitters Pain Relief Meds <ul><li>Substance P </li></ul><ul><li>Glutamate </li></ul><ul><li>GABA </li></ul><ul><li>Norepinephrine </li></ul><ul><li>Serotonin </li></ul><ul><li>Histamine </li></ul><ul><li>NSAIDS </li></ul><ul><li>Antidepressants </li></ul><ul><li>Anti seizure meds </li></ul><ul><li>Muscle relaxants </li></ul><ul><li>Local salves- capsaicin </li></ul><ul><li>Narcotics </li></ul>
  • 11. Body’s Natural Analgesia <ul><li>Activation by physical, chemical or threat of injury. </li></ul><ul><li>Nociceptive neurons release Substance P = pain! </li></ul><ul><li>Endogenous opioids are present at brain sites </li></ul><ul><ul><li>Released during stress, pain &amp; anticipation of pain to produce analgesia </li></ul></ul><ul><ul><li>Endorphins and enkephalins </li></ul></ul>
  • 12. Opioid Distribution in the Brain
  • 13. Location and time course of pain evoked neural activity in human subjects
  • 14. PET Scans show endogenous opioid activation during sustained pain
  • 15. &nbsp;
  • 16. Opioid Clinical Indications <ul><li>Analgesia </li></ul><ul><li>Acute Pulmonary Edema </li></ul><ul><li>Cough </li></ul><ul><li>Diarrhea </li></ul><ul><li>Anesthesia </li></ul>
  • 17. Pharmacologic Types of Opiates <ul><li>Natural Sources </li></ul><ul><ul><li>Opium, Morphine (10% of opium) </li></ul></ul><ul><ul><li>and Codeine (5%) </li></ul></ul><ul><ul><li>Heroin </li></ul></ul><ul><ul><ul><li>Morphine with 2-acetyl groups </li></ul></ul></ul><ul><ul><ul><ul><li>Heroin is a pro-drug: it is converted in the liver to morphine </li></ul></ul></ul></ul><ul><ul><ul><li>Sold as non-addictive </li></ul></ul></ul><ul><ul><ul><li>Dreser inventor of ASA </li></ul></ul></ul><ul><ul><ul><li>Banned in 1924 </li></ul></ul></ul>
  • 18. <ul><li>Synthetic Group </li></ul><ul><ul><li>Meperidine (Demerol)- short acting </li></ul></ul><ul><ul><li>Methadone (Dolophine)- orally effective </li></ul></ul><ul><ul><li>Hydromorphone (Dilaudid) </li></ul></ul><ul><ul><li>Pentazocine (Talwin) </li></ul></ul><ul><ul><li>Propoxyphene (Darvon) </li></ul></ul><ul><ul><li>Buprenorphine (Buprenex)- partial agonist </li></ul></ul><ul><ul><li>Oxycodone (Oxycontin, Percodan, Percocet) </li></ul></ul><ul><ul><li>Hydrocodone (Vicodin, Lorcet, Norco) </li></ul></ul>
  • 19. Drugs Methods of Use <ul><li>Oxycondone HCL </li></ul><ul><ul><li>Oxycontin, oxy, OC, killer </li></ul></ul><ul><li>Dilaudid, Percodan </li></ul><ul><ul><li>Dreamer, Junk </li></ul></ul><ul><li>Demerol, Morphine </li></ul><ul><li>Methadone </li></ul><ul><li>Heroin </li></ul><ul><ul><li>Smack, horse,bigH </li></ul></ul><ul><li>Codeine </li></ul><ul><ul><li>Schoolboy </li></ul></ul><ul><li>Swallowed, snorted, injected </li></ul><ul><li>Swallowed, inject </li></ul><ul><li>Injected, smoked, swallowed </li></ul>
  • 20. &nbsp;
  • 21. Oxycontin Abuse <ul><li>When tablets are crushed, snorted or extracted &amp; injected. </li></ul><ul><li>Effective, less toxic, well-tolerated medication. </li></ul><ul><li>Backlash ‘war on drugs’ challenges legitimate users </li></ul>
  • 22. &nbsp;
  • 23. Common Opioid Side Effects <ul><li>Constipation </li></ul><ul><li>Mental clouding, fatigue </li></ul><ul><li>Nausea, vomiting </li></ul><ul><li>Itch </li></ul><ul><li>Sweating </li></ul><ul><li>Urinary retention </li></ul>
  • 24. Symptoms of Use <ul><li>Drowsiness </li></ul><ul><li>Droopy Lids </li></ul><ul><li>Pin Point Pupils </li></ul><ul><li>Lethargy </li></ul><ul><li>Needle marks </li></ul><ul><li>Loss of appetite </li></ul><ul><li>Hazards of use is addiction with severe withdrawal symptoms </li></ul>
  • 25. &nbsp;
  • 26. Reinforcing Pharmacologic Properties <ul><li>Pain Relief </li></ul><ul><li>Change or elevate mood </li></ul><ul><li>Relieve tension, fear, anxiety </li></ul><ul><li>Produce feelings of peace, euphoria, tranquility </li></ul><ul><li>Rapid IV injection complete drive satiation </li></ul><ul><li>Why? </li></ul><ul><li>Most opioids increase DA activity! </li></ul>
  • 27. Poly Pharmacy
  • 28. Additive Toxicity Issues <ul><li>Tolerance </li></ul><ul><li>Dependence </li></ul><ul><ul><li>Physical </li></ul></ul><ul><ul><li>Psychological </li></ul></ul><ul><li>Overdose </li></ul><ul><li>Drug Interactions </li></ul><ul><li>Contraindications </li></ul>
  • 29. Acute Opioid Overdose <ul><li>Acute intoxication </li></ul><ul><li>Depressed BP &amp; Respiration </li></ul><ul><li>Fixed pinpoint pupil </li></ul><ul><li>Depressed sensorium </li></ul><ul><li>Coma, pulmonary edema </li></ul>
  • 30. Opioid Antagonists <ul><li>Pure Opioids Antagonist </li></ul><ul><ul><li>Naloxone (Narcan) </li></ul></ul><ul><ul><li>Naltrexone </li></ul></ul><ul><li>Mixed agonist – antagonist </li></ul><ul><ul><li>Nalorphine </li></ul></ul>
  • 31. Abstinence or Withdrawal Symptoms <ul><li>Related to the t 1/2 of the opioid in use </li></ul><ul><li>First 24 hrs. </li></ul><ul><ul><ul><li>Chills, hot flashes, restless sleep, piloerection on the skin (cold turkey), rhinorrhea, drowsiness, lacrimation, mydriasis </li></ul></ul></ul><ul><ul><ul><li>Sneezing, yawning, cramping, vomit, diarrhea, anorexia, increased BP, P, Temp, drug craving </li></ul></ul></ul><ul><ul><ul><li>If severe results in CV collapse </li></ul></ul></ul>
  • 32. Abstinence Syndrome <ul><li>Depending on agent </li></ul><ul><ul><li>Develops 2-48 hours </li></ul></ul><ul><ul><li>Peaks 72 hours </li></ul></ul><ul><ul><li>Untreated withdrawal may continue up to 7-10 days </li></ul></ul><ul><ul><li>Physical dependence is eventually lost </li></ul></ul><ul><ul><li>Psychological dependence continues longer or forever </li></ul></ul>
  • 33. Non-Opioid Withdrawal Treatments <ul><li>Clonidine (Catapres) </li></ul><ul><ul><li>Reduces SANs flow by stimulating alph receptors in the brain </li></ul></ul><ul><ul><li>Tablet- rapid </li></ul></ul><ul><ul><li>Patch- 2-3 days </li></ul></ul><ul><ul><ul><li>SE-sedative, hypotensive </li></ul></ul></ul><ul><li>Reduction </li></ul><ul><ul><li>HR, TPR, BP </li></ul></ul><ul><li>Withdrawal Programs </li></ul><ul><ul><li>Cold turkey? </li></ul></ul><ul><ul><li>Therapeutic </li></ul></ul><ul><li>Therapeutic Community Programs </li></ul><ul><ul><li>Goal relief from compulsive craving for the drug of abuse </li></ul></ul>
  • 34. Methadone <ul><li>Detox/ Withdrawal </li></ul><ul><ul><li>Cross-tolerance </li></ul></ul><ul><ul><li>No euphoria, rush </li></ul></ul><ul><li>Guide: </li></ul><ul><ul><li>1mg of methadone for: </li></ul></ul><ul><ul><ul><li>20 mg meperidine </li></ul></ul></ul><ul><ul><ul><li>4 mg morphine </li></ul></ul></ul><ul><ul><ul><li>2 mg heroin </li></ul></ul></ul><ul><ul><li>Methadone reduction 5mg increments </li></ul></ul><ul><li>Supportive Care </li></ul><ul><ul><li>Psychologic/Psychiatric </li></ul></ul><ul><li>25% continue Heroin </li></ul><ul><li>Maintenance </li></ul><ul><ul><li>Controversial </li></ul></ul><ul><ul><li>Requires Licensing </li></ul></ul><ul><ul><li>Hospital Environment </li></ul></ul><ul><ul><li>Goal complete w/drawal from drug dependency </li></ul></ul><ul><li>Methadone Dependence </li></ul><ul><ul><li>Less severe symptoms, lasts longer </li></ul></ul><ul><ul><li>Supplemental Rehabilitation </li></ul></ul>
  • 35. Additional Agonist Analgesics Use For Maintenance <ul><li>Buprenorphine/Naloxone (Suboxone) </li></ul><ul><ul><ul><li>Opioid agonist used in pain management and opiate dependence </li></ul></ul></ul><ul><ul><ul><li>Reduction in craving and increased success in abstinence programs </li></ul></ul></ul><ul><li>Levomethadyl Acetate (ORLAAM) </li></ul><ul><ul><ul><li>Longer acting alternative to methadone </li></ul></ul></ul><ul><ul><ul><li>Given three times a week </li></ul></ul></ul><ul><li>Diacetylmorphine (Heroin) </li></ul><ul><ul><ul><li>CI with no accepted medical use in the US </li></ul></ul></ul><ul><ul><ul><li>European hospitals and clinics </li></ul></ul></ul><ul><ul><ul><ul><li>For use with a history intractable dependence </li></ul></ul></ul></ul>
  • 36. &nbsp;
  • 37. Pain Syndromes <ul><li>Acute Pain  recent onset, transient, identifiable cause </li></ul><ul><li>Chronic Pain  persistent or recurrent pain, beyond usual course of acute illness or injury </li></ul><ul><ul><li>Nonmalignant </li></ul></ul><ul><ul><ul><li>Diagnosed or undiagnosed cause such as a nonmalignant disease </li></ul></ul></ul><ul><ul><li>Malignant </li></ul></ul><ul><ul><ul><li>Disease present pain severity worsens as progresses </li></ul></ul></ul><ul><li>Breakthrough Pain  transient pain, severe or excruciating, over baseline of moderate pain </li></ul>
  • 38. ABC’s of Pain Management Assess pain regulary Believe patients &amp; their families in their reports of pain Choose interventions appropriately Deliver these in a timely fashion Enable/Empower patients &amp; Families to overcome pain no pain mild discomforting horrible excruciating
  • 39. Pain Management
  • 40. Non-Drug Pain Management Techniques <ul><li>Distraction </li></ul><ul><ul><li>Ice/Heat </li></ul></ul><ul><ul><li>TV/ read/visiting </li></ul></ul><ul><li>Relaxation </li></ul><ul><ul><li>Breathing, yoga </li></ul></ul><ul><ul><li>Tapes, music </li></ul></ul><ul><li>Massage </li></ul><ul><li>Physical Therapy </li></ul><ul><li>Biofeedback </li></ul><ul><li>Acupuncture </li></ul><ul><li>Acupressure </li></ul><ul><li>Imagery </li></ul><ul><li>Aromatherapy </li></ul>
  • 41. Analgesic Ladder <ul><ul><li>NSAID (ASA) </li></ul></ul><ul><ul><li>Adjuvant analgesic (APAP, antihist) </li></ul></ul><ul><ul><li>Non-narcotic analgesic (NSAID) </li></ul></ul><ul><ul><li>Weak opioid (Codeine, propoxyphene) </li></ul></ul>Strong opioid (Morphine) with adjuvant analgesic
  • 42. PCA (patient-controlled analgesia pump)
  • 43. Why a Pump?

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