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Transcript
WR Fentanyl Symposium Opioids, Overdose, and Fentanyls WR Fentanyl Symposium Outline: What are opioids? Why are we experiencing and “opioid crisis”? Potency, purity, and product How do opioids cause overdose and overdose deaths? What is naloxone and how does it work? WR Fentanyl Symposium What is an opioid?: Any chemical that activates opioid receptors can be called an opioid, including: - chemicals produced in the human brain, e.g. endorphins - chemicals found in nature, e.g. morphine, codeine - modified versions of natural opioids, e.g. oxycodone, heroin - fully synthetic chemicals, e.g. fentanyl, meperidine WR Fentanyl Symposium What is an opioid receptor?: A protein found in many cell types, including brain cells, that interacts with opioids and mediates their effects The three main types of opioid receptors are: μ “Mu” δ “Delta” κ “Kappa” image.slidesharecdn.com/opioidreceptorsopioidanalgesics-160618124306/95/opioid-receptors-its-analgesics-23-638.jpg?cb=1466254016 WR Fentanyl Symposium Why fentanyls?: Fentanyl is a potent opioid, used in anesthesia, for pain, chronic pain, pain in end of life care Typically administered as a patch placed on the skin Fentanyl is produced by pharmaceutical manufacturers Small chemical changes to fentanyl can result in drugs with very similar actions These “bootleg” or “illicit” fentanyls are not produced in regulated manufacturing facilities WR Fentanyl Symposium https://www.google.ca/url?sa=i&rct=j&q=&esrc=s&source=images&cd WR Fentanyl Symposium Potency, purity, and product: Potency describes how much of a drug you need to get an effect Purity describes how much of the active opioid is present Product is what the patient or the user will use WR Fentanyl Symposium Why do we have an opioid crisis?: short answer :) North America has relatively high opioid prescribing rates We have manufactured products that are easy to use to achieve euphoria: OxyContin - could be crushed to get at high doses of oxycodone Fentanyl patches - 3 days worth of fentanyl could be extracted from a patch High strength opioids - contain a high dose of opioids per tablet or capsule WR Fentanyl Symposium Why do we have an opioid crisis?: (short answer!) North America has relatively high opioid prescribing rates We have manufactured products that are easy to use to achieve euphoria: X OxyContin - could be crushed to get at high doses of oxycodone Fentanyl patches - 3 days worth of fentanyl could be extracted from a patch High strength opioids - contain a high dose of opioids per tablet or capsule WR Fentanyl Symposium Why do we have an opioid crisis?: (short answer!) North America has relatively high opioid prescribing rates We have manufactured products that are easy to use to achieve euphoria: X X OxyContin - could be crushed to get at high doses of oxycodone Fentanyl patches - 3 days worth of fentanyl could be extracted from a patch High strength opioids - contain a high dose of opioids per tablet or capsule WR Fentanyl Symposium Why do we have an opioid crisis?: (short answer!) North America has relatively high opioid prescribing rates We have manufactured products that are easy to use to achieve euphoria: X X X OxyContin - could be crushed to get at high doses of oxycodone Fentanyl patches - 3 days worth of fentanyl could be extracted from a patch High strength opioids - contain a high dose of opioids per tablet or capsule WR Fentanyl Symposium What do opioids do?: Activation of opioid receptors leads to: - relief of pain and altered pain perception - sedation and anesthesia - cough suppression - constipation/treatment of diarrhea - miosis (small pupils) - euphoria - tolerance, dependence, addiction - nausea and vomiting - sweating - respiratory depression WR Fentanyl Symposium What do opioids do?: Activation of opioid receptors leads to: - relief of pain and altered pain perception - sedation and anesthesia - cough suppression - constipation/treatment of diarrhea - miosis (small pupils) - euphoria - tolerance, dependence, addiction - nausea and vomiting - sweating - respiratory depression WR Fentanyl Symposium What do opioids do?: Activation of opioid receptors leads to: - relief of pain and altered pain perception - sedation and anesthesia - cough suppression - constipation/treatment of diarrhea - miosis (small pupils) - euphoria - tolerance, dependence, addiction - nausea and vomiting - sweating - respiratory depression http://images.medicaldaily.com/sites/medicaldaily.com/files/styles/headline/public/2015/12/18/heroin.jpg WR Fentanyl Symposium What do opioids do?: Activation of opioid receptors leads to: - relief of pain and altered pain perception - sedation and anesthesia - cough suppression - constipation/treatment of diarrhea - miosis (small pupils) - euphoria - tolerance, dependence, addiction - nausea and vomiting - sweating - respiratory depression https://upload.wikimedia.org/wikipedia/commons/f/f0/Occhi222.jpg WR Fentanyl Symposium What do opioids do?: Activation of opioid receptors leads to: - relief of pain and altered pain perception - sedation and anesthesia - cough suppression - constipation/treatment of diarrhea - miosis (small pupils) - euphoria - tolerance, dependence, addiction - nausea and vomiting - sweating - respiratory depression https://lh5.googleusercontent.com/x18Lx7tc3BDy WR Fentanyl Symposium https://lh5.googleusercontent.com/x18Lx7tc3BDy WR Fentanyl Symposium Respiratory centre: Normally, the respiratory centre controls breathing without any conscious control When oxygen levels fall (and carbon dioxide levels start to rise) the respiratory centre causes you to breath more and rapidly When oxygen levels are high (and carbon dioxide levels are low) breathing slows WR Fentanyl Symposium Opioid receptors in the respiratory centre: Opioids interfere with respiratory centre function Over-activation of opioid receptors make the respiratory centre less and less sensitive to rising carbon dioxide levels in the blood Breathing becomes less frequent, more shallow, and ultimately stops during an opioid overdose WR Fentanyl Symposium Respiratory centre depression and the “safety window”?: All CNS depressants could potentially cause respiratory depression and death A key question for a specific drug is - how much do you need to treat pain or achieve euphoria vs. cause respiratory depression For potent opioids, the difference between these 2 amounts gets smaller, and smaller, and smaller: WR Fentanyl Symposium Opioid Effective Dose (pure product) Lethal Dose Morphine 10 mg 200 mg Fentanyl 0.1 mg 2 mg Carfentanil 0.001 mg 0.02 mg WR Fentanyl Symposium Naloxone: All opioids are opioid receptor AGONISTS (binds and activates the receptor) Naloxone is opioid receptor ANTAGONIST (binds, but does not activate the receptor naloxone morphine WR Fentanyl Symposium Opioid overdose: Lots of opioid over-activating the opioid receptors WR Fentanyl Symposium Naloxone reverses the overdose: By competing for opioid receptors and kicking off the opioid WR Fentanyl Symposium Naloxone doesn’t last long: Naloxone is metabolized faster than opioid agonists WR Fentanyl Symposium Naloxone metabolism: As naloxone levels fall, but the opioid remains, the overdoes could return