1. 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

2. 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 =
“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)