opioids Flashcards

(33 cards)

1
Q

what is opium

A

dries latex obtained from poppy

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2
Q

what are opiates

A

any drug derived from opium

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3
Q

what is an opioid

A

any drug that binds to an opioid receptor

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4
Q

what is a narcotic

A

illegal use of opioids for non-medical purposes

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5
Q

what kind of receptors are opioid receptors

A

Gi

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6
Q

what are the downstream effects of opioid receptors

A

inhibit calcium channels, activate K channel, inhibit adenylyl cyclase

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7
Q

what are the 4 types of opioid receptors

A

mu kappa delta ORL1

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8
Q

What affects does a mu opioid receptor agonist have

A

analgesia, reward, antitussive, respiratory depression, constipation

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9
Q

what affects does a mu opioid antagonist have

A

aversive, prevent reward, block overdose

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10
Q

what does a delta opioid agonist do

A

not rewarding, no analgesia, seizure inducing

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11
Q

what does a delta agonist do?

A

no obvious affects

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12
Q

what effects does a kappa agonist have

A

aversive, hallucinogenic, anxiogenic

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13
Q

what effects does a kappa antaonist have

A

antidepressent, anxiolytic

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14
Q

What kind of action does morphine have

A

full mu opioid receptor agonist

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15
Q

what kind of action does buprenorphine have

A

partial mu opioid agonist

antagonist at delta and kappa

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16
Q

what kind of action does methadone have

A

full mu opioid receptor agonist

17
Q

what kind of action does fentanyl have

A

full mu opioid receptor agonist

18
Q

what kind of action does heroin have

A

full mu opioid receptor agonist

19
Q

how do biased agonists work

A

arrests G protein signalling and activates its own

20
Q

what are beta-arrestins

A

blocks further G protein signalling

21
Q

what is UGT2B7

A

most important glucoronidation enzyme of morphine

22
Q

what metabolizes codeine into morphine

23
Q

what are the 3 endogenenous opioid peptides

A

beta endorphins, enkephalins, dynorphins

24
Q

describe the affinity of pro-enkephalin

A

delta»mu»kappa

25
what is the affinity of pro-opiomelanocortin
mu=delta>>kappa
26
what is the affinity of pro-dynorphin
kappa>>mu=delta
27
how do opioid receptors affect noxious inhibitory control
increase
28
how does opioid receptors affect the net nociceptive signals reaching the brain
reduction
29
how do opioids effect dopamine
increase (they inhibit the inhibitory GABAergic interneurons)
30
which agonists are being developved for migraines
delta opioid
31
what drug is being developed for migraine
TRV250 delta opioid biased agonist
32
what is CR845
analgesic, anit-inflammatory, anti itch
33
what is naloxone
non-selective competitive opioid receptor antagonist