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PMCOL 305 > opioid 2 > Flashcards

opioid 2 Flashcards

1
Q

what are the 4 distinct endogenous opioid-like substances

A

enkephalins
endorphins
endomorphins
dynorphins

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2
Q

what are the 3 opioid receptors

A

delta
mu
kappa

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3
Q

what is the main receptor for enkephalins

A

delta

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4
Q

what is the main receptor for endorphins

A

mu

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5
Q

what is the main receptor for endomorphins

A

mu

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6
Q

what is the main receptor for dynorphins

A

kappa

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7
Q

where do the endogenous opioid-like substances come from

A

different precursor proteins

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8
Q

what do all endogenous opioid-like substances CONTAIN and where

A

tyrosine at N terminus

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9
Q

what are 3 functions of endogenous opioid-like substances

A

neurotransmitters
neurohormones
neuromodulators

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10
Q

what are 4 things that endogenous opioid-like substances are involved in

A

pain
placebo response
acute stress response
social attachment

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11
Q

what kind of G protein is the opioid receptors

A

Gi

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12
Q

how many transmembrane domains in opioid receptors

A

7

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13
Q

what are mu receptors like (physically)

A

large, open binding pocked may allow for rapid exchange of ligans

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14
Q

what are 4 things mediated by mu receptors

A
  • euphoria
  • respiratory depression
  • analgesia
  • dependence
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15
Q

what is 1 thing mediated by the delta receptors

A

analgesia

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16
Q

what are 2 things mediated by kappa receptors

A

dysphoria, some analgesia

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17
Q

what are the 2 main things Gi does (not ion stuff)

A

inhibit adenylate cyclase

reduce cAMP

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18
Q

what are the 2 ions things Gi does

A

inhibit Ca++ influx

enhance K+ outflow

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19
Q

which type of Ca++ channels is inhibited by Gi

A

N type

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20
Q

what does K+ outflow do to membrane

A

hyperpolarization

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21
Q

what do opioids do to neuronal excitability

A

decrease

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22
Q

what do opioids do in the reward pathway

A

increase DA in NAc by inhibiting GABA induced inhibition

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23
Q

how do opioids increase DA in NAc

A

by inhibiting GABA induced inhibition

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24
Q

why do some studies show that there isnt much of a increase in DA in addicts (like 3 flaws in the studies)

A
  • they used subQ injections
  • individuals were on methadone
  • people were addics
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25
Q

what is the % DA increase with morphine in opioid-naive individuals

A

400%

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26
Q

what are the things you get physiologically tolerant to with opioids

A

analgesia, vomiting, euphoria, respiratorry depression

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27
Q

what are the things you dont get physiologically tolerant to with opioids

A

constipation and pupil constriction

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28
Q

what kind of dose over baseline can addicts take with little respiratory depression

A

50X!

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29
Q

what is biased agonism

A

when one agonist preferentially activates certain signalling pathways while another at the same receptor preferentially activates different pathways

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30
Q

what are 2 examples of biased agonism

A

G-protein mediated and beta-arrestin mediated

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31
Q

what do different biased agonists do to the receptor

A

stabilize different receptor conformations that interact with different proteins

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32
Q

what happens to activated receptors

A

they are phosphorylated by kinases

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33
Q

what attracts beta-arrestin

A

activated receptors

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34
Q

what do beta-arrestins do

A

inhibit G-protein signalling to prevent further activation of pathways

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35
Q

what happens to receptors bound to beta-arrestins

A

they can be removed from the membrane or participate in other signalling pathways

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36
Q

which pathway does morphine favor (beta-arrestins or G protein)

A

G-protein

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37
Q

which pathway does fentanyl favor (beta-arrestins or G protein)

A

beta-arrestin

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38
Q

what degree of phosphorylation for G-protein pathway

A

low

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39
Q

what degree of phosphorylation for beta-arrestin

A

high

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40
Q

which pathway has a low degree of phosphorylation

A

G-proteins

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41
Q

which pathway has a high degree of phosphorylation

A

beta-arrestin

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42
Q

what 4 effects are the beta-arrestin pathway

A

down-regulation
side effects
tolerance
dependence

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43
Q

what are the beta-arrestin subtypes

A

1 2 3 4

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44
Q

what does GRK do

A

add phosphate groups (kinase) to agonist-bound receptors

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45
Q

what does GRK stand for

A

G-protein related kinase

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46
Q

what happens to tolerance and side effects with beta-arrestin knock out

A

less side effects and tolerance

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47
Q

what happens to tolerance and side effects with drugs that favor the G protein path

A

less side effects and tolerance

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48
Q

what happens to receptors with short term opioid exposure

A

the receptors are internalized but recycled to the surface in minutes or hours

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49
Q

what happens to receptors with long term opioid exposure

A

they are internalized and destroyed

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50
Q

does morphine or fentanyl cause more receptor degradation and why

A

fentanyl cause it activates beta-arrestins instead of G proteins

51
Q

what are 3 things beta-arrestin binding causes (after G receptor activation and GPCR phosphorylation)

A
  • block further G protein signalling
  • redirects signalling to its own alternative pathway
  • targets receptors for internalization
52
Q

if G protein does more the analgesic effect, what effects do the beta arrestins cause

A

respiratory depression, tolerande, bad GI, insufficient analgesia

53
Q

if beta arrestins cause respiratory depression, tolerande, bad GI, insufficient analgesia,
what do the G proteins do

A

analgesia

54
Q

what causes hyperalgesia with long term treatment of opioids (4)

A

increase adenylyl cyclase, PKC PKS and NMDA

55
Q

what does the NDMA upregulation in long term opioids do

A

causes hyperexcitable to pain

56
Q

why does cell make more adenylyl cyclase with long term opioids

A

to try to make more cAMP (opioids are Gi)

57
Q

what composes the opioid overdose triad

A

coma
depressed respiration
pinpoint pupils

58
Q

what % of overdose deaths had another depressant in them

A

85%

59
Q

what % of overdose deaths had a benzo in them

A

45%

60
Q

what % of overdose deaths had alcohol in them

A

36%

61
Q

what is naloxone

A

fast acting opioid antagonist

62
Q

how long does naloxone last

A

20-40 minutes

63
Q

what can naloxone reverse

A

resp depression
coma
miosis
death

64
Q

what happens if you give naloxone to someone who is using opioids

A

it will precipitate withdrawal

65
Q

what happens if you give naloxone to someone who doesnt use opioids

A

no significant effects

66
Q

how fast can you get opioid withdrawal symptoms

A

four hours or less after previous use

67
Q

how fast can you feel quite ill after using opioids

A

608 hours

68
Q

how many injections of opioids do you need daily to stop feeling ill

A

3-4

69
Q

why do they feel so much pain in opioid withdrawal

A

because your Body starts to upregulate pain pathways

70
Q

what correlates with intensity and duration of withdrawal symptoms

A

intensity and duration of drugs effect

71
Q

what kind of withdrawal for heroin

A

intense but short

72
Q

what kind of withdrawal for methadone

A

mild but prolonged

73
Q

what are the first symptoms for withdrawal

A

cravings for drugs, anxiety

74
Q

what are the 2nd symptoms for withdrawal

A

yawning
sweating
tearing eyes
running eyes

75
Q

what are the 3rd symptoms for withdrawal

A

2nd + pupil dilation, goosebumps, cold hot flashes, aching, appetite loss

76
Q

what are the 4th symptoms for withdrawal

A

3rd + insomnia high BP high temp high BP respiration nausea

77
Q

what are the 5th symptoms for withdrawal

A

4th+curled up position, vomiting, diarrhea, weight loss, spontaneous ejaculation, increased blood sugar

78
Q

what does chronic opioid use do to NA release and how

A

less NA release because it suppresses firing rate of adrenergic neurons in locus coeruleus

79
Q

what happens to NA firing in tolerance and how

A

it normalizes because it up-regulates adenylyl cycles and PKA production

80
Q

what happens to NA production when opioids are removed and why

A

massive NA release and withdrawal symptoms due do hyperactive adrenergic neurons in locus coeruleus

81
Q

what may cause many of the withdrawal symptoms

A

the massive NA release when you stop taking opioids

82
Q

what are 8 symptoms of the massive NA release with withdrawal

A 
chills
sweating
stomach cramps
diarrhea
emesis
muscle pain
runny nose
runny eyes
83
Q

what happens with cAMP levels when you take opioids acutely

A

decrease at first

84
Q

what happens with cAMP levels when you take opioids after awhile

A

they slowly start to rise as your body upregulates other processes

85
Q

what is clonidine

A

alpha-2 agonist

86
Q

what is lofexidine

A

alpha-2 adrenergic agonist

87
Q

how do alpha-2 agonists work

A

prevent NA release from locus coeruleus

88
Q

where are alpha2 receptors (where in neuron)

A

presynaptic (autoreceptors)

89
Q

where are alpha2 receptors (where in brain that affect withrawal)

A

locus coeruleus

90
Q

does clonidine and lofexidine address the psychological issues of withdrawal

A

no

91
Q

what are the 2 alpha agonists used for withdrawal

A

clonidine and lofexidine

92
Q

what is a physical side effect of clonidine and lofexidine

A

low BP

93
Q

what stage of withdrawal is clonidine and lofexidine used for

A

detox

94
Q

what can clonidine and lofexidine be used alongside with

A

methadone or buprenorphine

95
Q

what is the class of opioid of methadone (natural synthetic)

A

synthetic

96
Q

what is the half life of methadone compared to heroin

A

longer

97
Q

why is methadone good

A

clean pure free, longer half life

98
Q

is methadone euphoric

A

yes but not a lot compared to heroin

99
Q

does methadone still cause constipation

A

yes :(

100
Q

what is the mode of consumption of methadone

A

oral

101
Q

what is another effect of methadone besides opioid

A

NMDA glutamate antagonist

102
Q

what does methadone do to NMDA

A

antagonize

103
Q

what is the mechanism of action of buprenorphine

A

partial agonist

104
Q

what is the class of opioid of buprenorphine (natural synthetic)

A

semi-synthetic

105
Q

what receptors does buprenorphine target the most

A

mu

106
Q

what is the half life of buprenorphine

A

37 hours

107
Q

how many doses per week of buprenorphine is needed

A

1-3

108
Q

what is the affinity to mu of buprenorphine vs heroin

A

higher affinity

109
Q

does buprenorphine have strong effects at mu receptor

A

no but it has a high affinity

110
Q

can you get respiratory depression with buprenorphine and why

A

not really cause its just a partial agonist

111
Q

what does buprenorphine do to the effects of heroin and how

A

blocks because it has a higher affinity at mu receptors

112
Q

does buprenorphine cause constipation

A

yes in some people

113
Q

is buprenorphine better than methadone

A

yes

114
Q

why is buprenorphine better than methadone

A
  • lower OD risk
  • lower recreational use
  • better tolerability
115
Q

whats suboxone

A

buprenorphine and naloxone (4:1)

116
Q

how is suboxone administered

A

sublingually

117
Q

what happens when suboxone is taken sublingually

A

naloxone has no effect and the partial agonist effects of buprenorphine are felt

118
Q

what happens when suboxone is taken via injection

A

naloxone will cause withdrawal effects

119
Q

how can a patient taking suboxone cause rapid withdrawal symptoms

A

if the patient isnt in active withdrawal (taking an agonist, they will go from 100-50% and feel terrible)

120
Q

why do patients have to be in active withdrawal to take suboxone

A

taking suboxone would cause rapid withdrawal symptoms (cause its a partial agonist)

121
Q

which drugs will have an effect with subligual use in suboxone

A

buprenorphine only (not naloxone)

122
Q

which drugs will have an effect with IV use in suboxone

A

naloxone prevents buprenorphine effects so it causes withdrawal

123
Q

how does suboxone get absorbed

A

mucosal membranes

124
Q

do all agonists cause the same degrees of G-protein effects or b-arrestin

A

no, diff agonists cause diff degrees of these effects

PMCOL 305 (26 decks)

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