Opioid Definition Flashcards
What does the term opioid refer to
Opiates
Derived compounds
Natural and synthetic analogs
Endogenous opioids
Endorphins
Dynorphins
Enkephalins
Opiates example
Morphine
Codeine
Semisynthetic opioids example
Buprenorphine
Heroin
Oxycodone
Fully synthetic opioids example
Fentanyl
Methadone
What does endogenous mean
Natural opioids
Three receptors of opioids
Mu
Kappa
Delta
Which receptor are we mostly worried about
Mu
Location of Mu receptors
Brain regions : pain , respiration , and reward system
Spinal cord
GI system
Peripheral regions
Prefrontal cortex Mu receptors function
Executive functioning
Thalamus mu receptors binding
Pain receptor - analgesia
Part of the Brain that is associated with euphoria (mu receptors activation)
NAc and VTA
What happens when mu receptors are activated in CNS
Analgesia effect
Sedation
Euphoria
Pupil constriction (small)
Decrease : RR and HR
Nausea
Body response to mu receptor activation in gut
Decrease mobility - constipation
Positive reinforcement with Opioids
Opioids cause dopamine to release in the brainstem.
Our bodies like them
Seek out more opioids to get that reward feeling again
Negative reinforcement from Opioid usage
Decrease utilization of the amygdala blunts are ability to fear, become anxious or stress.
Opioid usage on PFC
When Opioids bind to the mu receptors of PFC, our ability to have executive function decreases.
We make bad decisions.
What causes vulnerability to SUDs
50/50
Part: Genetics
Part: Environment
Full agonist
Completely binds to the receptor and activates it. Mimicks the NTs
Full antagonist
Completely blocks receptors to not activate them (Reuptake Inhibitors)
How does Naloxone bind to mu receptors
It acts as a full antagonist blocking the receptor
How does Buprenorphine bind to mu receptors.
It is a partial agonist. It slightly activates the receptors but does not bind to all of them
What is an example of a full agonist for Mu receptors
Methadone, Fentanyl, Morphine
How does Buprenorphine work
It allows for some activation of Mu receptors, however, it can block of other portion of receptors as well. It is a maintenance drug.
What type of class is Buprenorphine in
III
It is allowed office base (DATA 2000)
How does precipitated withdrawal occur
A partial agonist (Buprenorphine as high affinity for receptors) knocks off full agonist from receptor causing a dip in activation.
“The partial agonist always win, do NOT decrease or d/c.”
It is important to discuss timing. Risk of too much agonist on receptors before the addition of a partial agonists.
How does Naltrexone work:
Naltrexone blocks agonist for attaching to those mu receptors. Antagonist is out front like a goalie blocking the drug or NT to get into goal.
Use baseball analogy:
Agonist - fully in glove tight
partial agonist - in glove but not as tight
Antagonist: - Goalie, not in glove
Tolerance
Needing more to produce the same effect
Sx that develop from rapid tolerance
Euphoria
Analgesia
Nausea
Decreased respiration
Sx that develop from little to no tolerance
Constipation
Pin point eyes
How to lose tolerance
To go without that substance for a long time.
Often achieved in detox or with naltrexone usage.
What does Opioid intoxication look like
Everything drops:
Low RR and HR
Hypotension
Hypothermia
Sedation
Slowed movement
Slurred speech
Pinpoint eyes
Lower pain and stress
What does Opioid Overdose look like
Loss of consciousness
Pinpoint eyes
Decreased RR
No breathing
Treatment for Opioid Overdose
Narcan
Withdrawal
Abrupt stop of Opioids
s/s of withdrawal
Everything goes faster:
Elevated HR
High blood pressure
Increased temp
Sweating
Runny Nose
GI issues (Cramps, diarrhea, nasuea)
Pupil dilation
Muscle spasms
Onset of withdrawal for short acting Opioids
6 - 12 Hours
Symptom peaks for short acting opioids
36 - 72
How long is withdrawal for short acting opiods
roughly 5 days
example of short acting opioids
Oxy, heroine
Example of long acting opiods
Methadone
Onset of withdrawal for long acting opioids
36 - 48
Symptom peak for long acting opioids
72 hours
Duration of withdrawal for long acting opioids
up to 3 weeks
