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Pharmacology 200 > 2 opiods > Flashcards

2 opiods Flashcards

1
Q

what is opium

A

dried latex obtained from the poppy

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2
Q

what is opiates

A

any drug derived from opium

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3
Q

what are opioids

A

any drug that binds to an opiod receptor

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4
Q

are all opiates opioids

A

yes, even synthetic ones

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5
Q

what are narcotics

A

origionally for any drug with sleep inducing properties, but now used by law enfocement to talk about illegal use of opiods for non medical purposed

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6
Q

what kind of opiate is morphine

A

natural opiate

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7
Q

what kind of opiate is heroin

A

semisynthetic opiate (synthesized from morphine)

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8
Q

what kind of opiate is fentanyl

A

not an opiate, its just an opioid

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9
Q

how many times to GPCRs span the membrane

A

7 times

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10
Q

where are the N and C terminuses for GPCRs

A

N outside

C inside

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11
Q

which terminus binds the ligand

A

N

it outside

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12
Q

which terminus binds the effectors and like G protein stuff

A

C terminus

inside

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13
Q

what kind of G pathway are opiod receptors

A

Gi

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14
Q

what does activation of opioid receptors cause (3 direct + 1 overall)

A

inhibit calcium channels
activate K+ channels
inhibit adenylyl cylase

neuronal inactivation and reduced transmitter release

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15
Q

what are the four types of opioid receptors

A

mu
delta
kappa
ORL-1

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16
Q

what type of G proteins are the 4 types of opioid receptors

A

all Gi

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17
Q

what causes the 4 types to be different

A

due to receptor distribution differences (diff neurons, diff brain circuits)

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18
Q

what part of the opioid receptors differ the most

A

near the N and C terminus

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19
Q

whats a ligand

A

a molecule which binds a protein (receptor) to produce a biological effect
agonists or antagoinsts

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20
Q

what does mu agonism cause

A

analgesia, reward, antitissive, resp depression, constipation

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21
Q

example of mu agonist

A

morphine fentanyl heroin

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22
Q

what does mu antagonism cause

A

prevent reward, block overdose, aversive

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23
Q

example of mu antagonist

A

naloxone

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24
Q

what does delta agonism cause

A

not reward, no analgesia (yes migraine and chronic pain), some cause seizures

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25
Q

what does delta antagonism cause

A

no obvious effects

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26
Q

what does kappa agonism cause

A

aversive, hallucinogenic, anxiogenic

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27
Q

example of kappa agonist

A

salvia

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28
Q

what does kappa antagonism cause

A

potential antidepressant, anxiolytic

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29
Q

example of kappa antagonist

A

buphrenorphine

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30
Q

what does ORL-1 agonism cause

A

block opioid analgesia (no current theuraputic use)

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31
Q

what does ORL-1 antagonism cause

A

no obvious effects

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32
Q

what are 4 full mu opioid receptor agonists

A

morphine
methadone
fentanyl
heroin

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33
Q

what is 1 partial mu opioid receptor agonist

A

CODEINE

so its safer therapeutic index

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34
Q

why is codeine safer than morphine
methadone
fentanyl
heroin

A

it is a partial agonist instead of a full agonist

mild to moderate analgesic efficacy, safer therapeutic index

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35
Q

what differs between full agonists

A

they have different potencies (fentanyl more potent than morphine, but full agonists)

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36
Q

does efficacy or potency effect analgesia, euphoria, respiratory depression

A

both!

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37
Q

which receptors does buprenorphine affect

A

partial agonist at mu opioid receptor and antagonist at delta and kappa

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38
Q

what does buprenorphine do

A

treatment for pain and opioid addiction (opioid agonist therapy)

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39
Q

what are arrestins

A

family of proteins important for regulating signal transduction at GPCRs

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40
Q

what signal causes β-arrestin to bind

A

after receptor activation and G-protein cleavage, GPCR is phosphorylated and causes β-arrestin to bind

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41
Q

whats does β-arrestin cause

A

blocks further G-protein signalling, redirects signalling to alternative pathways, and targets receptors for internalization

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42
Q

do all opioid ligands lead to β-arrestin recruitment

A

not all
different opioid ligands can differently activate G-protein versus β-arrestin signaling pathways

some are balances, some are biased towards G protein or β-arrestins

these signalling pathways drive different aspects of the drug

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43
Q

what does the G-protein signalling pathway drive in mu opiod receptor

A

drives analgesia

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44
Q

what does the β-arrestins signalling pathway drive in mu opiod receptor

A

drives respiratory depression and GI function

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45
Q

what are two ways that the G protein biased agonist do their thing

A

the pathway drives analgesia AND since β-arrestins stop analgesia, inhibiting β-arrestins causes an extra increased analgesia

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46
Q

how are mu agonist opioids absorbed when taken orally

A

most are well absorbed

47
Q

which opioid undergoes extensive first-pass metabolism

A

morphine

48
Q

which opioid bypasses extensive first-pass metabolism

A

codeine

49
Q

how does opioids affect neonates

A

they cross the placental, effect fetus that can cause respiratory depression and physical dependence

50
Q

how are opioids agonists distributed through the body

A

widely distrubuted through the tissues, especially in highly perfused tissues (brain, lungs, kidney, spleen, liver)

51
Q

what is morphine metabolized by and into

A

by CYP2D6 and into M3G & M6G (morphine-3-glucuronide and morphine-6-glucuronide) (way more powerful)

52
Q

what is codeine metabolized by and into

A

CYP2D6

morphine

53
Q

what does genetic polymorphisms of CYP2D6 cause

A

fast or slow metabolizes

linked to variation in analgesic and adverse responses, especially in codeine

54
Q

can heroin pass the BBB and why

A

no because there is an acetyl group

55
Q

what does plasma esterases

A

it rapidly converts heroin into morphine, which easily corsses BBB

56
Q

how are polar metabolites excreted

A

in the urine

57
Q

what are the glucoronide conjugates

A

M3G and M6G

58
Q

how are M3G and M6G excreted

A

in the urine

59
Q

why do you have to worry with patients with renal impairment

A

active polar metabolites (M6G) cause even more sedation and resp. depression because they are not able to pee it out

60
Q

what are the three types of endogenous opioid peptides

A

endorphines
enkephalins
dynorphins

61
Q

which receptors do endogenous opioid peptides bind to

A

all opioid receptors

but with different affinities

62
Q

which receptor do endorphins bind best at

A

mu

63
Q

which receptor do enkephalins bind best at

A

delta

64
Q

which receptor do dynorphins bind best at

A

kappa!!

65
Q

what are the roles of the endogenous opioids

A

mediate variety pf behavioural effects like pain, reward, learning, memory and cognition

66
Q

how do endogenous opioids become themselves

A

they come from polepeptide precursors and are cleaved by distinct proteases (trypsin like)

67
Q

what is the claustrum

A

tiny brain region that connects to many regions of the cortex (visual, auditory, somatosensory, limbic)

integrates sensory information, maybe causes consciousness

68
Q

what is special with nerves in claustrum

A

3 neurons that extensively span the brain, 1 that wraps around the entire circumference of the brain like a crown of thorns

69
Q

what does stimulation of the claustrum cause

A

blocks volitile behaviour, unresponsiveness, amnesia, lost consciousness, no impact on motor skills

70
Q

what kind of receptors is the highest density in the claustrum

A

kappa opioid receptors

71
Q

why does kappa agonism cause hallucinogenic effects

A

because most kappa in claustrum which is connected to consciousness

72
Q

is codeine an opiate

A

yes

73
Q

what are the main functions of the opioid receptors in the brain

A

pain perception, reward, emotion, addiction

74
Q

what does opioid activity in the brainstem cause

A

it can cause respiratory depression

75
Q

what does opioid activity in the spinal cord cause

A

transmission of pain signals is dampened, especially the dorsal horn (receive sensory input)

76
Q

what does opioid activity in the peripheral neurons cause

A

curb pain sensation because of sensory neurons being bound to opioids

77
Q

what does opioid activity in the intestine cause

A

blocks peristalsis, causes constipation

78
Q

which receptors are used for pain

A

mu opioid agonists

79
Q

which receptors are used for migraine

side effects

A

delta opioid

seizure

80
Q

what would be some clinical benefits of kappa agonists

A

analgesic, anti-inflammatory, anti-itch, no CNS effects

81
Q

which horn receives sensory input

A

dorsal horn

82
Q

how is pain detected in the skin

A

C fiber primary afferent neurons

83
Q

where do C fiber primary synapse onto

A

secondary afferents in the dorsal horn in the spinal cord

84
Q

what is the role of secondary afferents

A

carry nociceptive information up to the brain

85
Q

are mu opioid receptors are localized on primary or secondary afferents?

A

both

86
Q

what does activation of mu opioid receptors does to pain

A

inhibits pain transmission from skin to brain

87
Q

what is the role of opioid receptors on the brainstem (PAG and medulla)

A

increase descending noxious inhibitory control

inhibit pain signal at the level of the spinal cord

88
Q

what is the rule of dopamine

A

motivational behaviour

89
Q

where are the neurons primarily located

A

ventral tegmental area (VTA)

90
Q

where are mu opioid receptors in the VTA located on

A

inhibitory GABAergic interneurons

91
Q

what is disinhibition

A

opioid inhibit inhibition, which leads to dopamine release

92
Q

how does opioid cause dopamine release

A

disinhibition

93
Q

what are the two ways that mu opioid receptors inhibit pain

A

decrease nociception at C fiber

decrease emotional and cognitive aspects of pain

94
Q

what makes the best analgesic

A

drugs that target the sensory, cognitice and emotional circuits

95
Q

what is the catch-22 of making a good pain relief

A

the best ones are also rewarding (and addicting!)

the analgesic and euphoric system overlap, hard to remove one without the other

96
Q

what is loperamide

A

mu agonist used for diarrhea

inhibits peristalsis and secretion

97
Q

what are the targets of loperamide (where located-specific)

A

mu opioid on cholinergic neurons of the gastrointestinal tract

98
Q

why isnt loperamide addicting

A

p-glycoprotein pumps it out from the brain

99
Q

what happens if you block p-glycoproteins

A

increase brain concentration of loperaminde

100
Q

what kind of drugs are dangerous to combine with loperamide

A

tricyclic antidepressants

101
Q

how does desensitization happen after using opioids

A

beta arrestin is recruited to shut off signalling, receptor removed from membrane

102
Q

what are the circuitry adaptations to opioids

A

increased pain, diarrhea, anxiety

103
Q

what are the metabolic adaptations to opioids

A

upregulation of enzymes that metabolize the drugs

104
Q

is dependence the same as addiction

A

no

addiction is more extreme, its more about the behaviour

105
Q

what is addiction

A

a brain disease driven by dysfunction in reward, motivation and memory circuitry. inability to abstain, cant control behaviour

106
Q

are all drug dependent users addiction

A

no

107
Q

are all addicted drug users dependent

A

yes

108
Q

how do drug companies try to prevent drug abuse

A

make them non crushable

make prodrug that must be metabolized in GI (cant be bypassed by intravenous use)

109
Q

what is agonist replacement therapy

A

maintenance on an opioid agonist (buprenorphine, methadone) and CBT

110
Q

what is buprenorphine

A

partial mu opioid agonist and kappa antagonist

111
Q

what is methadone

A

long lasting full agonist at the mu receptor (24-42 hrs)

112
Q

what is naloxon

A

non-selective competitive opioid receptor antagonist

113
Q

how do opioids increase dopamine release

A

disinhibition of GABAergic inhibitory tone on dopaminergic neuronal cell bodies in the VTA

Pharmacology 200 (29 decks)

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