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Pharmacy Intro

Pharmacy Intro. Opioids and other drugs we use on palliative care. Objectives. Discuss the role of opioids in end of life care Discuss the pharmacology and side effects of opioids Discuss opioid equivalencies and conversions Review basics of methadone Discuss other medications commonly used.

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Pharmacy Intro

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  1. Pharmacy Intro • Opioids and other drugs we use on palliative care

  2. Objectives • Discuss the role of opioids in end of life care • Discuss the pharmacology and side effects of opioids • Discuss opioid equivalencies and conversions • Review basics of methadone • Discuss other medications commonly used

  3. Objectives (cont’d) • Discuss other medications commonly used

  4. Barriers to opioid use • Physician • Patient

  5. Why use opioids • Pain is experienced by over 80% of patients • Over 60% will be moderate to severe • Dyspnea present in 80% of advanced cancer • 95% COPD at end of life • 75% of advanced disease (all comers)

  6. Opioids in Canada

  7. Opioid Pharmacokinetics • All have similar PK (except methadone) • onset of action 15-30 mins • duration of action 4-5 hrs • LA 8-12hrs

  8. Opioid Pharmacokinetics • Fentanyl and Sufentanil • Onset 10-15 mins • Duration 45 mins • First pass metabolism • Highly lipophilic (SL/IN)

  9. Opioid Dosing • No ceiling effect • ↑dose = ↑analgesic effect (log-linear) • Dose increased until symptom relief or limiting side effects

  10. Start with IR dosing • “Start Low and Go Slow” • Q4H • PO = SL = PR • SC/IV = 50% of PO • Reassess regularly

  11. Breakthrough Dose • IR • 50-100% of the Q4H dose or 10% of the 24hr dose • Q1H - PO/SL • Q30Min - SC • Q10Min - IV • For simplicity... all routes are Q1H prn

  12. Do Not Use Extended Release Opioid for Breakthrough

  13. Titration • Increase equal to total 24 hours breakthrough dose • Mild to moderate pain - 50% • If no response • Increase more rapidly • Switch to parenteral

  14. Opioid Rotation • Why? • Inadequate analgesia despite appropriate escalation • Intractable/Intolerable side effects • Altered renal/hepatic function • Drug shortages

  15. Use a consistent method • Use the same conversion table • Consider incomplete cross-tolerance, patient variations, limitation of tables

  16. Equianalgesia Dose Ratio • Equianalgesia refers to different doses of two agents that provide approximate pain relief • Does not reflect interpatient variability • Ratio differs in acute and chronic use • Does not use incomplete cross tolerance

  17. Opioid Equivalency

  18. Fentanyl

  19. Fentanyl Patch • For relatively stable pain • Permeates the skin and a depot is formed • 12hrs to develop analgesia • Plasma levels stabilize after 2 sequential patch applications • Half-life about 17 hours after removal

  20. Methadone • Opioid agonist (mu, kappa, delta) • N-methyl-d-aspartate (NMDA) antagonist • Inhibits reuptake of serotonin and noradrenalin • Nociceptive and neuropathic pain

  21. Analgesic effect 30-60mins • Duration 4-6hrs • T1/2 8-100+ hrs (~30hrs) • Peak 1.5-3hrs • Large Vd, 80% bioavailability, large protein binding • Accumulates in chronic use • Metabolized in liver, eliminated in urine and feces • Multiple drug interactions

  22. Side Effects of Opioids • Nausea (50-70%) and Vomiting (15-20%) • Constipation • Sedation • Confusion • Respiratory depression • Urinary retention • Pruritus • ↑ Qt with methadone

  23. Other Medications (our cheat sheet)

  24. Questions

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