close VGCC in presynaptic terminals reducing NT release; open K+ channels in postsynaptic cells inhibiting AP transmission
What is the MOA of opioids? (2)
a
Which pathway do opioids cause inhibition?
a) ascending pathway
b) descending pathway
b
Which pathway do opioids cause activation?
a) ascending pathway
b) descending pathway
increase dopamine release in nucleus accumbens; through inhibition of GABAnergic neurons
How do Opioids influence the Reward Pathway?
brain stem; medulla
Respiratory depression occurs through the inhibition of the _________
respiratory center; cough suppression occurs through decreased cough
reflex in the ________.
miosis, constipation
Which effects of opioids will NOT succumb to tolerance? (2)
peripheral vasodilation and hypotension
How do opioids affect the CV system?
plasma esterases, Hepatic P450
What are the two primary modes of metabolism in Opioids?
CYP3A4
Fentanyl is metabolized by _________.
codeine, oxycodone, hydrocodone
Which Opioids are metabolized by CYP2D6? (3)
loss of function
What is the most common polymorphism in CYP2D6?
2-3 weeks into chronic administration
When does tolerance usually develop?
receptor downregulation-overexposure to opioids; anti-opiate chemicals- block G protein activity
What are the potential mechanisms for developing Opioid tolerance? (2)
MOR agonists of the same class
Which drugs can become susceptible to cross-tolerance?
b,d
Which drugs can exhibit withdrawal symptoms the fastest?
a) Meperidine
b) Heroin
c) Methadone
d) Morphine
c
Which has the least intense withdrawal symptoms?
a) Meperidine
b) Heroin
c) Methadone
d) Morphine
48 hours
When do physical withdrawal symptoms generally peak?
1 week
When do physical symptoms start to lessen?
2 weeks
When do psychological symptoms peak?
months
How long can psychological symptoms persist?
a
Which is used for cough?
a) Codeine
b) Methadone
c) Fentanyl
d) Buprenorphine
e) Meperidine
f) Loperamide
g) Dipneyoxylate/atropine
f,g
Which are used for diarrhea?
a) Codeine
b) Methadone
c) Fentanyl
d) Buprenorphine
e) Meperidine
f) Loperamide
g) Dipneyoxylate/atropine
c
Which is used for anesthesia?
a) Codeine
b) Methadone
c) Fentanyl
d) Buprenorphine
e) Meperidine
f) Loperamide
g) Dipneyoxylate/atropine
b,d
Which are used for opioid use disorder?
a) Codeine
b) Methadone
c) Fentanyl
d) Buprenorphine
e) Meperidine
f) Loperamide
g) Dipneyoxylate/atropine
e
Which is used for postanesthetic shivering?
a) Codeine
b) Methadone
c) Fentanyl
d) Buprenorphine
e) Meperidine
f) Loperamide
g) Dipneyoxylate/atropine
naloxone, naltrexone
Which drugs are used for Opioid overdose? (2)
Methylnaltrexone bromide, Naloxegol, naldemedine
What are the Peripherally-acting Mu-Opioid Antagonists (PAMORAS) (3)
codeine, oxycodone, dihydrocodeine, hydrocodone, diphenoxylate, loperamide
What are the mild-moderate MUR agonists? (6)
buprenorphine, butorphanol, Nalbuphine, Pentazocine
Which MUR agonists have Mixed-Receptor actions? (4)
morphine, hydromorphone, oxymorphone, methadone, -tanil, meperidine, levorphanol
What are the strong MUR Agonists? (7)
constipation, slows peristalsis, increased water reabsorption, urinary retention
What are the GI effects of Opioids? (4)
analgesia, euphoria, dysphoria, sedation, opioid-induced hyperalgesia, respiratory depression, cough suppression, miosis
What are the CNS effects of Opioids? (7)
testosterone, libido, energy, mood
Opioids can agonize HPA hormones causing a decrease in what?
c
Which receptor is responsible for causing respiratory depression?
a) Delta
b) Kappa
c) Mu
b
Which receptor is responsible for causing dysphoria?
a) Delta
b) Kappa
c) Mu
a
Which receptor is responsible for anti-depression?
a) Delta
b) Kappa
c) Mu
c
Which receptor is found in the GI?
a) Delta
b) Kappa
c) Mu
constipation, urinary retention, immune system modulation, pruritus
What are AE's that occur in the periphery? (4)
tramadol, tapentadol
Which opioids are MUR agonists and NE reuptake inhibitors? (2)
to increase GI motility after bowel surgery
What is the use of Alvimopan?
partial; higher
Buprenorphine is a ______ agonists, but has _______ binding affinity than other MUR agonists.
d
Which is resistant to Naloxone reversal?
a) Codeine
b) Methadone
c) Fentanyl
d) Buprenorphine
e) Meperidine
f) Loperamide
g) Dipneyoxylate/atropine
b
Which is more potent?
a) Naloxone
b) Naltrexone
b
Which can cause hepatotoxicity?
a) Naloxone
b) Naltrexone
a
Which is used in combination with Buprenorphine?
a) Naloxone
b) Naltrexone
a
Which can also antagonize Kappa & Delta receptors?
a) Naloxone
b) Naltrexone
treatment of OUD, alcohol use disorder
What is the CA of Naltrexone? (2)
reversal of opioid effects
What is the CA of Naloxone?
a
Which has a shorter DoA and rapid binding?
a) Naloxone
b) Naltrexone