Nagelhout Video's- Opioid Agonists/Antagonists Flashcards
What are the 3 endogenous groups of opioids
Enkephalins
Endorphins
Dynorphins
What is the oral form of narcan?
Naltrexone
Which opioid receptor is responsible for dysphoria?
Kappa
Which opioid receptor has an anti-shivering effect?
Kappa
What would happen if you gave buprenorphine to someone after giving them morphine?
Their pain would get worse (agonist/antagonist or partial agonist)
> alone, this drug will give some analgesia, but if given after a more potent analgesic it will result in increased pain
Buprenorphine (pronounced ‘bew-pre-nor-feen’
what does alkaloid in chemistry mean?
naturally occurring, comes from a plant and has pharamacologic effects
phenanthrene alkaloid prototypes (2)
Morphine, Codeine
(naturally occuring)`
Semi-synthetic phenanthrene alkaloids (5)
HHHO
Heroin
Hydrocodone (Vicodin)
Hydromorphone (Dilaudid)
Oxycodone (Oxycotin)
Phenylpiperidines protype (1)
+4
meperidine (Demerol)
(fentanyl, su, al, remi)
If your allergic to a phenanthrene… are you allergic to all phenanthrenes?
Yes!
But your not allergic to the phenylipiperidines or the methadones
T/F- all the phenanthrenes cause histamine release
True AND Demerol
List the potency of opioids from weakest to strongest:
Remi
Fentanyl
Su
Meperidine
Alfentanil
Morphine
Hydromorphone
Meperidine (0.1)
Morphine (1)
Hydromorphone (7)
Alfentanil (10)
Remi (100)
Fentanyl (100)
Sufentanil (1000)
How to remember potency of fentanyl family:
AR Fifteen’S
Al Remi Fent Su
What is remi metabolized by?
Nonspecific esterases in the plasma
What’s special about codeine?
It’s not an active drug. It’s a prodrug- meaning it becomes active once it’s in the body and it becomes metabolized to it’s active form – morphine and it’s actually morphine that relieves the pain (0.4x less potent then actual morphine)
Why can’t you give codeine to kids?
Because if they are fast metabolizers, they will produce higher levels of morphine than expected and it can lead to respiratory depression
What is demerol metabolized to?
What’s the concern?
Who should it be avoided in?
Normerperidine
*lowers the seizure threshold! and increases CNS excitability
*HD and old peeps (cant pee out the metabolite)
Any patient on what kind of drug cannot receive demerol?
What drugs fall under this category 5()
MAOi’s
Isocarboxizid
Phenelzine
Tranylcypromine
Selegiline
Rasagiline
(seizures, severe cardiac issues)
Why does remifentanil have a low Vd if it’s very lipophilic?
Because it’s metabolized in the plasma before it can distribute to other compartments.
What opioid is based on Lean Body weight and why?
3 other drugs based on LBW we use
Remifentanil
-because despite it being lipophilic, it behaves like a drug that has a low Vd bc it is rapidly metabolized in the plasma. So the extra fat someone has doesn’t matter.
[vec/roc/cist]
Duration of remifentanil (hours and minutes)
0.1 hour
= 6 minutes
One reason you want to front load your opioids
Because the most stimulating aspects of surgery are at the beginning –> #1 intubation, #2 skin incision
skin closure is the least stimulating
Opioids shift the CO2 response curve to the right or left
Right
(fancy way of saying the cause respiratory depression)
> minute ventilation is lower than expected for a given CO2 level
What’s the purpose of lowering the resp rate at the end of the case?
To build up CO2 - opioids shift the CO2 response curve to the right, so it’s going to take a higher CO2 than normal to stimulate them to breathe
If opioids don’t have a direct effect on BP, why do we give it during the case when the BP goes up?
Because your treating the sympathetic response to pain and when the pain goes away, the blood pressure drops.