Pharmacology of Opioids (1) C.L.I.P.S. Receptors & effect involved in opioid function Mu - analgesia, sedation, euphoria, respiratory depression, constipation, and physical dependence Delta – mild analgesia and less respiratory depression Kappa – analgesia with fewer adverse effects Agonists morphine, fentanyl, oxycodone, hydrocodone, methadone activate mu receptors, producing analgesia Partial agonists Buprenorphine strong affinity for mu receptors, but produces mild analgesia that is accompanied by an analgesic ceiling effect strong affinity may displace other mu receptor agonists Agonist-Antagonist pentazocine, butorphanol (Stadol), nalbuphine (Nubain) antagonists on mu receptors and as agonists on kappa receptors, leading to milder analgesic effects with fewer adverse effects Antagonists naloxone and naltrexone block mu and kappa receptor activation, preventing analgesia; they are used mostly as reversal agents What receptor is likely responsible for addiction despite all the SE on the back? Mu receptor (likely through the cause of euphoria) 2/16 Matel

What is mechanism of opioid overdose and death? Risks of Long Term Opioids(2) C.L.I.P.S. Who is at risk of unintentional overdose and death? MED > 120 per day Maybe MED > 90 per day per CDC **Anyone on opioids and benzos** (only use with extreme caution) Calculate MED = http://agencymeddirectors.wa.gov/mobile.html “Opioid” App for Apple (“Opioid converter” Android) Other risks of long term opioid use (at any dose) Respiratory - Respiratory depression, OSA Endocrine - decreased bone density, amenorrhea, galactorrhea, decreased testosterone - > erectile dysfunction CNS effects – fatigue, drowsiness, confusion Cardiac - Prolonged QT, hypotension Pruritus Urinary retention GI – constipation, N/V (cyclic vomiting) Hyperalgesia, allodynia Dry mouth/tooth decay Signs of opioid overdose Pinpoint pupils unconsciousness Respiratory depression What is mechanism of opioid overdose and death? Respiratory depression (cofounded by confusion/ drowsiness/ Sedatives)