Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
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 |