opioids Flashcards

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

A

CYP2D6

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
Q

what is the affinity of pro-opiomelanocortin

A

mu=delta»kappa

26
Q

what is the affinity of pro-dynorphin

A

kappa»mu=delta

27
Q

how do opioid receptors affect noxious inhibitory control

A

increase

28
Q

how does opioid receptors affect the net nociceptive signals reaching the brain

A

reduction

29
Q

how do opioids effect dopamine

A

increase (they inhibit the inhibitory GABAergic interneurons)

30
Q

which agonists are being developved for migraines

A

delta opioid

31
Q

what drug is being developed for migraine

A

TRV250 delta opioid biased agonist

32
Q

what is CR845

A

analgesic, anit-inflammatory, anti itch

33
Q

what is naloxone

A

non-selective competitive opioid receptor antagonist