Hosam Mohamed-
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
