Pharmacology_2 14: Opiates

Front 1

3 natural opiates

Back 1

morphine
codeine
thebaine

Front 2

3 families of opioids in decreasing order of peptide length

Back 2

beta-endorphins
dynorphins
enkephalins

Front 3

beta-endorphin is more/less potent than morphine when injected intracerebrally

Back 3

more

Front 4

___ antagonizes beta-endorphin

Back 4

naloxone

Front 5

endorphin release is triggered by ___ (3)

Back 5

stress
electrical stimulation
acupuncture

Front 6

stimulation of ___ (2) triggers endorphin release

Back 6

periaqueductal grey
substantia gelatinosa

Front 7

opioid receptor ___ aka ___ is the receptor bound by most opioids
it causes ___ (3)

Back 7

mu
OP3
analgesia
GI transit
respiratory depression

Front 8

opioid receptor ___ aka ___ causes ___ (2)

Back 8

kappa
OP2
visceral pain analgesia
abstinence syndrome (?)

Front 9

buprenorphine is a partial agonist of ___, an agonist of ___, and an antagonist of ___
naloxone antagonizes receptors ___

Back 9

mu
delta
kappa
mu, kappa, delta

Front 10

___ is the strongest kappa agonist
___ is the weakest

Back 10

oxycodone
methadone

Front 11

all opiod Rs are ___s and signal via ___

Back 11

GPLRs
G_i

Front 12

opioid Rs increase ___ current and decrease ___ current. this causes ___ polarization

Back 12

K+
Ca2+
hyper

Front 13

in brainstem, opioids work by ___ing the ___ of ___ neurons

Back 13

inhibiting
inhibitor neuron
pain inhibitor

Front 14

opiate receptors on ___s (2) decrease afferent pain

Back 14

nociceptor
projection neuron

Front 15

T/F: opioid receptors are present at distal nociceptor terminals

Back 15

true

Front 16

5 CNS side effects of opioids

Back 16

euphoria
diminished respiratory drive
nausea
miosis
sedation

Front 17

miosis from opioids is due to stimulation of ___, from which ___ emerges

Back 17

Edinger-Westphal nucleus
CN 3

Front 18

3 endocrine side effects of opioids

Back 18

reduced ACTH
reduced GnRH
increased PRL

Front 19

rarely, opiods cause ___

Back 19

convulsions

Front 20

4 opioid GI side effects

Back 20

diminished secretion
increased sphincter tone
increased muscle contractility
altered peristalsis

Front 21

2 urinary opioid side effects

Back 21

inhibition of voiding reflex
increased sphincter tone

Front 22

2 peripheral opioid side effects

Back 22

HA release
vasodilation

Front 23

5 opioids for mild/moderate pain

Back 23

propoxyphen
codeine
tramadol
buprenorphine
pentazocine

Front 24

propoxyphen has a long/short t1/2 and is metabolized by ___. it is related to ___

Back 24

long
liver
methadone

Front 25

codeine is ___ as potent as morphine. it is partially metabolized to ___

Back 25

1/10
morphine

Front 26

tramadol is a ___ analogue
it is ___ as potent as morphine
tramadol blocks reuptake of ___ (2) but doesn't work as ___

Back 26

codeine
1/5
NE
5-HT
antidepressant

Front 27

buprenorphine is ___ as potent as morphine
it is not antagonized by ___
it can be given ___ly

Back 27

25--50 times
naloxone
transdermally

Front 28

___ is the active metabolite of morphine and accumulates in ___

Back 28

M6G
renal failure

Front 29

IV morphine is ___ times more potent than oral

Back 29

3

Front 30

oxycodone has greater/smaller bioavailability than morphine

Back 30

smaller

Front 31

to prevent constipation, oxycodone is given with ___.

Back 31

naloxone

Front 32

naloxone has higher/lower R affiinity than oxycodone

Back 32

higher

Front 33

in the liver, oxycodone is ___ and naloxone is ___. therefore, ___ is active in the body.

Back 33

not metabolized
metabolized
oxycodone

Front 34

fentanyl is ___ as potent as morphine.
it has ___ onset and duration
it is given ___ly (2)

Back 34

100 times
short
transdermally
transbuccally

Front 35

methadone acts as a ___ agonist and ___ antagonist. it can be given ___ly (2)

Back 35

mu
NMDA
orally
epidurally

Front 36

as methadone dose increases, methadone/morphine analgesic ratio ___s

Back 36

increases

Front 37

meperidine has long/short duration
it is given ___ly
it has a potentally fatal interaction with ___s

Back 37

short
by injection
MAOI

Front 38

tolerance develops to ___ (2)

Back 38

analgesia
side effects

Front 39

abstinence syndrome can be caused by ___ (2)

Back 39

dose reduction
antagonist

Front 40

2 causes of tolerance/dependance

Back 40

upregulation of receptors for nociceptive neurotransmitters
desensitization of opioid receptors

Front 41

___ is an opioid which suppresses cough

Back 41

dextromethorphan

Front 42

___ is a kappa agonist

Back 42

enkephalin

Front 43

meperidine is aka ___
trade name is ___
like methadone, it ___s
unlike methadone, it ___s

Back 43

pethidine
demerol
agonizes mu
agonizes delta, kappa

Front 44

meperidine is stronger/weaker than morphine
it is used for ___ because ___

Back 44

weaker
biliary colic
causes less GI & biliary spasticity

Front 45

opioids inhibit release of ___ (4 neurotrans)

Back 45

ACh
NE
5-HT
Glu
substance P

Front 46

codeine is aka ___

Back 46

methylmorphine

Front 47

3 partial mu agonists
these can cause ___ in people who ___

Back 47

buprenorphine
butorphanol
pentazocine
abstinence syndrome
are on full mu agonists

Front 48

butorphanol is used for ___, especially ___
it causes less ___ than full mu agonists

Back 48

pain
migraine
respiratory depression

Front 49

pentazocine is used for ___

Back 49

moderate/severe pain

Front 50

3 endocrine side effects of opioids

Back 50

decreased ACTH
decreased GnRH
increased PRL

Front 51

___ can be co-administered with oxycodone to counteract GI side effects

Back 51

naloxone

Front 52

___ is an opioid antagonist used to treat alcohol dependence
it is also used for ___

Back 52

naltrexone
opioid dependence

Front 53

naltrexone blocks ___ (2) receptors

Back 53

mu
kappa

Front 54

tx for opioid withdrawal (2)

Back 54

buprenorphine + naloxone
methadone

Front 55

buprenorphine preparations for tx of opioid dependence include ___
the reason is ___
the preparation is called ___

Back 55

naloxone
naloxone will antagonize mu Rs if the preparation is injected (abused) and will induce withdrawal sx
suboxone