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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
    • Opium
      • The sap of the seed pod of Papaver somniferum, referred to as early as 3000 BC.
      • Found in Spanish burial sites c.4200 BC
    • Greeks/Romans
      • Used to produce constipation, sleep, panacea
      • God Morpheus (God of Dreams)
  • 5.  
  • 6. Recent History
  • 7.  
  • 8.  
  • 9. Opioids (God Morpheus of Dreams) Narcotics (Narcosis—stupor)
    • Produce analgesia by binding to opiate receptors in the CNS, brain and spinal cord involved with the transmission of pain impulses.
    • Produce Morphine like effects on the opioid receptors
  • 10. Pain Neuro Transmitters Pain Relief Meds
    • Substance P
    • Glutamate
    • GABA
    • Norepinephrine
    • Serotonin
    • Histamine
    • NSAIDS
    • Antidepressants
    • Anti seizure meds
    • Muscle relaxants
    • Local salves- capsaicin
    • Narcotics
  • 11. Body’s Natural Analgesia
    • Activation by physical, chemical or threat of injury.
    • Nociceptive neurons release Substance P = pain!
    • Endogenous opioids are present at brain sites
      • Released during stress, pain & anticipation of pain to produce analgesia
      • Endorphins and enkephalins
  • 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.  
  • 16. Opioid Clinical Indications
    • Analgesia
    • Acute Pulmonary Edema
    • Cough
    • Diarrhea
    • Anesthesia
  • 17. Pharmacologic Types of Opiates
    • Natural Sources
      • Opium, Morphine (10% of opium)
      • and Codeine (5%)
      • Heroin
        • Morphine with 2-acetyl groups
          • Heroin is a pro-drug: it is converted in the liver to morphine
        • Sold as non-addictive
        • Dreser inventor of ASA
        • Banned in 1924
  • 18.
    • Synthetic Group
      • Meperidine (Demerol)- short acting
      • Methadone (Dolophine)- orally effective
      • Hydromorphone (Dilaudid)
      • Pentazocine (Talwin)
      • Propoxyphene (Darvon)
      • Buprenorphine (Buprenex)- partial agonist
      • Oxycodone (Oxycontin, Percodan, Percocet)
      • Hydrocodone (Vicodin, Lorcet, Norco)
  • 19. Drugs Methods of Use
    • Oxycondone HCL
      • Oxycontin, oxy, OC, killer
    • Dilaudid, Percodan
      • Dreamer, Junk
    • Demerol, Morphine
    • Methadone
    • Heroin
      • Smack, horse,bigH
    • Codeine
      • Schoolboy
    • Swallowed, snorted, injected
    • Swallowed, inject
    • Injected, smoked, swallowed
  • 20.  
  • 21. Oxycontin Abuse
    • When tablets are crushed, snorted or extracted & injected.
    • Effective, less toxic, well-tolerated medication.
    • Backlash ‘war on drugs’ challenges legitimate users
  • 22.  
  • 23. Common Opioid Side Effects
    • Constipation
    • Mental clouding, fatigue
    • Nausea, vomiting
    • Itch
    • Sweating
    • Urinary retention
  • 24. Symptoms of Use
    • Drowsiness
    • Droopy Lids
    • Pin Point Pupils
    • Lethargy
    • Needle marks
    • Loss of appetite
    • Hazards of use is addiction with severe withdrawal symptoms
  • 25.  
  • 26. Reinforcing Pharmacologic Properties
    • Pain Relief
    • Change or elevate mood
    • Relieve tension, fear, anxiety
    • Produce feelings of peace, euphoria, tranquility
    • Rapid IV injection complete drive satiation
    • Why?
    • Most opioids increase DA activity!
  • 27. Poly Pharmacy
  • 28. Additive Toxicity Issues
    • Tolerance
    • Dependence
      • Physical
      • Psychological
    • Overdose
    • Drug Interactions
    • Contraindications
  • 29. Acute Opioid Overdose
    • Acute intoxication
    • Depressed BP & Respiration
    • Fixed pinpoint pupil
    • Depressed sensorium
    • Coma, pulmonary edema
  • 30. Opioid Antagonists
    • Pure Opioids Antagonist
      • Naloxone (Narcan)
      • Naltrexone
    • Mixed agonist – antagonist
      • Nalorphine
  • 31. Abstinence or Withdrawal Symptoms
    • Related to the t 1/2 of the opioid in use
    • First 24 hrs.
        • Chills, hot flashes, restless sleep, piloerection on the skin (cold turkey), rhinorrhea, drowsiness, lacrimation, mydriasis
        • Sneezing, yawning, cramping, vomit, diarrhea, anorexia, increased BP, P, Temp, drug craving
        • If severe results in CV collapse
  • 32. Abstinence Syndrome
    • Depending on agent
      • Develops 2-48 hours
      • Peaks 72 hours
      • Untreated withdrawal may continue up to 7-10 days
      • Physical dependence is eventually lost
      • Psychological dependence continues longer or forever
  • 33. Non-Opioid Withdrawal Treatments
    • Clonidine (Catapres)
      • Reduces SANs flow by stimulating alph receptors in the brain
      • Tablet- rapid
      • Patch- 2-3 days
        • SE-sedative, hypotensive
    • Reduction
      • HR, TPR, BP
    • Withdrawal Programs
      • Cold turkey?
      • Therapeutic
    • Therapeutic Community Programs
      • Goal relief from compulsive craving for the drug of abuse
  • 34. Methadone
    • Detox/ Withdrawal
      • Cross-tolerance
      • No euphoria, rush
    • Guide:
      • 1mg of methadone for:
        • 20 mg meperidine
        • 4 mg morphine
        • 2 mg heroin
      • Methadone reduction 5mg increments
    • Supportive Care
      • Psychologic/Psychiatric
    • 25% continue Heroin
    • Maintenance
      • Controversial
      • Requires Licensing
      • Hospital Environment
      • Goal complete w/drawal from drug dependency
    • Methadone Dependence
      • Less severe symptoms, lasts longer
      • Supplemental Rehabilitation
  • 35. Additional Agonist Analgesics Use For Maintenance
    • Buprenorphine/Naloxone (Suboxone)
        • Opioid agonist used in pain management and opiate dependence
        • Reduction in craving and increased success in abstinence programs
    • Levomethadyl Acetate (ORLAAM)
        • Longer acting alternative to methadone
        • Given three times a week
    • Diacetylmorphine (Heroin)
        • CI with no accepted medical use in the US
        • European hospitals and clinics
          • For use with a history intractable dependence
  • 36.  
  • 37. Pain Syndromes
    • Acute Pain  recent onset, transient, identifiable cause
    • Chronic Pain  persistent or recurrent pain, beyond usual course of acute illness or injury
      • Nonmalignant
        • Diagnosed or undiagnosed cause such as a nonmalignant disease
      • Malignant
        • Disease present pain severity worsens as progresses
    • Breakthrough Pain  transient pain, severe or excruciating, over baseline of moderate pain
  • 38. ABC’s of Pain Management Assess pain regulary Believe patients & their families in their reports of pain Choose interventions appropriately Deliver these in a timely fashion Enable/Empower patients & Families to overcome pain no pain mild discomforting horrible excruciating
  • 39. Pain Management
  • 40. Non-Drug Pain Management Techniques
    • Distraction
      • Ice/Heat
      • TV/ read/visiting
    • Relaxation
      • Breathing, yoga
      • Tapes, music
    • Massage
    • Physical Therapy
    • Biofeedback
    • Acupuncture
    • Acupressure
    • Imagery
    • Aromatherapy
  • 41. Analgesic Ladder
      • NSAID (ASA)
      • Adjuvant analgesic (APAP, antihist)
      • Non-narcotic analgesic (NSAID)
      • Weak opioid (Codeine, propoxyphene)
    Strong opioid (Morphine) with adjuvant analgesic
  • 42. PCA (patient-controlled analgesia pump)
  • 43. Why a Pump?