L? Pharm of opiates - Barker Flashcards
two types of alkaloids that opium contains
phenanthrenes
benzylisoquinolines
what are the 3 non-phenanthrene opioids ***
tramadol
meperidine
fentanyl
(all others are phenanthrenes im pretty sure)
T or F: sigma receptors are opioid receptors
false
Opioid receptor signal transduction:
Presynaptic: inhibit _____ channel (Gi), decrease in ________ releas
calcium
neurotransmitter
Opioid receptor signal transduction:
Postsynaptic: Activate ______ channel (GBy) -> Efflux of ___ leading to hyperpolarization
GIRK
K+
T or F: Opioid induced side effects are mostly on-target effects **
True
T or F: Pruritus is an allergic response due to opioids, not a side effect
false, other way around
7 side effects induced by opioids
resp depression
constipation
Pruritus
Addiction
urinary retention
N/V
Miosis
T or F: Kappa opioid receptor has potential use for treatment of addiction due to its increase in dopamine release
false, reduction
3 therapeutic uses of mu opioid receptor *
analgesia (not as effective for chronic pain)
sedation
antitussive (cool)
Endogenous opioid for mu opioid receptor ***
endorphin
M-morphine
Which opioid receptor some verb counterbalance mu opioid receptor effects
kappa
which opioid receptor?
Dynorphins natural ligand
- preprodynorphin
kappa
natural ligand for delta opioid receptor
Enkephalins
- preprronekphalin
T or F: Delta opioid receptors are extracellular
false, intracellular
Which opioid receptor has a role in hypoxia/ischemia/stroke ?
delta
Which opioid receptor reduces anxiety and depression?
delta
which of the opioid receptors can treat alcoholism?
delta.
one listed side effect on delta opioid receptor slide
seizures
T or F: There are no FDA approved Kappa opioids
False, its no delta
Opioid site of action:
_______ -> _________
ventral tegmental area -> nucleus accumbens
make sure you actually look at the MOA on slide 16
okay please do it cole i beg you
which opioid has first pass metabolism with a bioavailability of 25%?
morphine
Morphine CYP(s)
2d6 and 3a4
Morphine:
MOA (kinda):
Phen or nonphen:
Receptor:
NMDA activity?
Kappa activity?
full agonist
phen
mu
no nmda
no kappy
Nociceptin receptor endogenous opioid
nociceptin duh
which 3 opioids are prodrugs with an active metabolite? *
heroin
codeine
tramadol
T or F: Fentanyl and methadone produce active metabolites
False
High lipophilicity
A. Morphine
B. Fentanyl
b
CYP3A4 makes opioids starting with?
NOR
oxycodone -> noroxycodone
oxymorphone -> noroxymorphone
PM (poor metabolizer) (of CYP2D6) phenotype is more common in what group?
white people somehow
__ phenotype is of high relevance worldwide.
A. PM (poor)
B. IM (intermediate)
C. EM (extensive)
D. UM (ultra-rapid)
D
fentanyl is how much more potent than:
morphine
heroin
100 x
50 x
which opioid is typically used in palliative care
fentanyl
which 3 opioids are broken down by plasma esterases due to ester linkage?
3 synthetic ones: sufentanil, remifentanil, alfentanil
which opioid has snri properties?
tramadol
which opioid has the toxic active metabolite normeperidine?
meperidine (demerol) lol
Methadone: **
- Primarily used for ______ ________
- ________ __ (unwanted effect)
- ______ antagonist *
opioid dependence
prolonged QTc
NMDA
2 opioids that can be used for cough
codeine and dextromethorphan
2 opioid agonists used as anti-diarrheal
Diphenoxylate w/ atropine (lomotil)
and
loperamide (imodium)
Pentazocine and Butorphanol MOA
Kappa agonist, partial agonist/antagonism at mu
3 side effects for pentazocine and butorphanol
less dysphoria
hallucinations
increase in BP/HR
Nalbuphine (nubain) MOA
Full agonist at kappa
antagonist at mu
antagonism produces withdrawal
buprenorphine MOA and primary use
Partial mu agonist, weak kappa agonist and delta antagonist (damn)
primary use in opioid replacement therapy
3 meds used for preventative and acute mgmt of ileus and constipatino
senna -> colonic contraction** (so pick this one if it comes up)
miralax
docusate
Methadone MOA
FULL mu agonist
T or F: Methadone is frequently used in medication assisted treatment for opioid dependence
true.
T or F: Methadone is fast acting and has less accumulation
False, slow acting and accumulates with repeated dose
what is the buprenorphine and naloxone combo called?
suboxone
T or F: Subutex has abuse potential.
true
T or F: Naltrexone has decent oral bioavailability
true
2 opioid antagonists
naloxone and naltrexone
which opioid antagonist is typically given IV or intranasal
naloxone
short half life (30-90 min)
A. Naloxone
B. Naltrexone
A
how long after the first narcan (naloxon) dose should you give the second?
2-5 minutes IF NOT CONSCIOUS
4 sxs of neonatal abstinence syndrome
tremors
yawning
poor feeding
sweating
T or F: Heroin, methadone, and other opiates can cause serious withdrawal in babies when born
true
Seizures may also be a sx of neonatal abstinence syndrome in babies born to _____ users *
methadone
5 options for non-pharm tx of neonatal abstinence syndrome *
swaddling
hypercaloric formula
frequent feedings
observation
rehydration
(all easy i guess)
Pharmacological tx of neonatal abstinence syndrome (3.5)
morphine sulfate
sublingual buprenorphine
methadone
maybe clon?
Which 2 tx options are linked to a shorter hospital stay than methadone in the tx of neonatal abstinence syndrome?
morphine and buprenorphine
