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55 Cards in this Set

  • Front
  • Back
3 natural opiates
morphine
codeine
thebaine
3 families of opioids in decreasing order of peptide length
beta-endorphins
dynorphins
enkephalins
beta-endorphin is more/less potent than morphine when injected intracerebrally
more
___ antagonizes beta-endorphin
naloxone
endorphin release is triggered by ___ (3)
stress
electrical stimulation
acupuncture
stimulation of ___ (2) triggers endorphin release
periaqueductal grey
substantia gelatinosa
opioid receptor ___ aka ___ is the receptor bound by most opioids
it causes ___ (3)
mu
OP3
analgesia
GI transit
respiratory depression
opioid receptor ___ aka ___ causes ___ (2)
kappa
OP2
visceral pain analgesia
abstinence syndrome (?)
buprenorphine is a partial agonist of ___, an agonist of ___, and an antagonist of ___
naloxone antagonizes receptors ___
mu
delta
kappa
mu, kappa, delta
___ is the strongest kappa agonist
___ is the weakest
oxycodone
methadone
all opiod Rs are ___s and signal via ___
GPLRs
G_i
opioid Rs increase ___ current and decrease ___ current. this causes ___ polarization
K+
Ca2+
hyper
in brainstem, opioids work by ___ing the ___ of ___ neurons
inhibiting
inhibitor neuron
pain inhibitor
opiate receptors on ___s (2) decrease afferent pain
nociceptor
projection neuron
T/F: opioid receptors are present at distal nociceptor terminals
true
5 CNS side effects of opioids
euphoria
diminished respiratory drive
nausea
miosis
sedation
miosis from opioids is due to stimulation of ___, from which ___ emerges
Edinger-Westphal nucleus
CN 3
3 endocrine side effects of opioids
reduced ACTH
reduced GnRH
increased PRL
rarely, opiods cause ___
convulsions
4 opioid GI side effects
diminished secretion
increased sphincter tone
increased muscle contractility
altered peristalsis
2 urinary opioid side effects
inhibition of voiding reflex
increased sphincter tone
2 peripheral opioid side effects
HA release
vasodilation
5 opioids for mild/moderate pain
propoxyphen
codeine
tramadol
buprenorphine
pentazocine
propoxyphen has a long/short t1/2 and is metabolized by ___. it is related to ___
long
liver
methadone
codeine is ___ as potent as morphine. it is partially metabolized to ___
1/10
morphine
tramadol is a ___ analogue
it is ___ as potent as morphine
tramadol blocks reuptake of ___ (2) but doesn't work as ___
codeine
1/5
NE
5-HT
antidepressant
buprenorphine is ___ as potent as morphine
it is not antagonized by ___
it can be given ___ly
25--50 times
naloxone
transdermally
___ is the active metabolite of morphine and accumulates in ___
M6G
renal failure
IV morphine is ___ times more potent than oral
3
oxycodone has greater/smaller bioavailability than morphine
smaller
to prevent constipation, oxycodone is given with ___.
naloxone
naloxone has higher/lower R affiinity than oxycodone
higher
in the liver, oxycodone is ___ and naloxone is ___. therefore, ___ is active in the body.
not metabolized
metabolized
oxycodone
fentanyl is ___ as potent as morphine.
it has ___ onset and duration
it is given ___ly (2)
100 times
short
transdermally
transbuccally
methadone acts as a ___ agonist and ___ antagonist. it can be given ___ly (2)
mu
NMDA
orally
epidurally
as methadone dose increases, methadone/morphine analgesic ratio ___s
increases
meperidine has long/short duration
it is given ___ly
it has a potentally fatal interaction with ___s
short
by injection
MAOI
tolerance develops to ___ (2)
analgesia
side effects
abstinence syndrome can be caused by ___ (2)
dose reduction
antagonist
2 causes of tolerance/dependance
upregulation of receptors for nociceptive neurotransmitters
desensitization of opioid receptors
___ is an opioid which suppresses cough
dextromethorphan
___ is a kappa agonist
enkephalin
meperidine is aka ___
trade name is ___
like methadone, it ___s
unlike methadone, it ___s
pethidine
demerol
agonizes mu
agonizes delta, kappa
meperidine is stronger/weaker than morphine
it is used for ___ because ___
weaker
biliary colic
causes less GI & biliary spasticity
opioids inhibit release of ___ (4 neurotrans)
ACh
NE
5-HT
Glu
substance P
codeine is aka ___
methylmorphine
3 partial mu agonists
these can cause ___ in people who ___
buprenorphine
butorphanol
pentazocine
abstinence syndrome
are on full mu agonists
butorphanol is used for ___, especially ___
it causes less ___ than full mu agonists
pain
migraine
respiratory depression
pentazocine is used for ___
moderate/severe pain
3 endocrine side effects of opioids
decreased ACTH
decreased GnRH
increased PRL
___ can be co-administered with oxycodone to counteract GI side effects
naloxone
___ is an opioid antagonist used to treat alcohol dependence
it is also used for ___
naltrexone
opioid dependence
naltrexone blocks ___ (2) receptors
mu
kappa
tx for opioid withdrawal (2)
buprenorphine + naloxone
methadone
buprenorphine preparations for tx of opioid dependence include ___
the reason is ___
the preparation is called ___
naloxone
naloxone will antagonize mu Rs if the preparation is injected (abused) and will induce withdrawal sx
suboxone