OPIOIDS Flashcards

1
Q

what are opioid drugs, what do they do

A

narcotic analgesics

reduce pain without producing unconsciousness

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2
Q

main ingredient in opium

A

morphine

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3
Q

how was heroin made

A

adding two acetyl groups to morphine, making it more lipid soluble

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4
Q

what are the benefits of heroin + mechanisms of action

A

reaches the brain faster
more potent than morphine
carrier molecule, acetyl groups cleave off when in brain.

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5
Q

opioid drugs bind to specific receptors in the ____, discovered using ________

A

brain, radio ligand assays

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6
Q

4 types of opioid receptors

A

mu, delta, kappa, NOP-R

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7
Q

what type of receptor are opioid receptors

A

G-protein linked metabotropic receptors

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8
Q

mu receptor has _____ affinity for _____

A

high, morphine

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9
Q

which areas cause analgesia due to mu receptor (5 areas)

A

medial thalamus, periaqueductal gray, raphe, locus coeruleus, spinal cord

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10
Q

Brainstem mu receptor binding causes what

A

cardiovascular/respiratory control, cough control, nausea/vomitting

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11
Q

sensorimotor integration mu receptor locations

A

thalamus, striatum

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12
Q

NAc Mu receptor effect

A

feeding, positive reinforcement , pleasurable aspects of fatty/sweet foods.

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13
Q

S (delta receptor) location

A

forebrain structures

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14
Q

delta receptor roles

A

olfaction, motor integration, reinforcement and cognitive function and overlap with mu receptors suggest modulation of analgesia.

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15
Q

K-(kappa) receptors location

A

striatum, amygdala, hypothalamus

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16
Q

kappa receptor role

A

regulation of pain perception, gut motility, and dysphoria

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17
Q

FQ receptors location + function

A

wide distribution (cortex, limbic areas, thalamus, raphe nuclei, spinal cord)
Does not bind opioid drugs
lowers pain thresholds
role in feeding, learning, motor function, reward and neuroendocrine regulation

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18
Q

first peptide transmitter that binds to opioid receptors

A

enkephalin

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19
Q

another endogenous peptide that binds to opioid receptors

A

endorphins

20
Q

how are endogenous opioid receptors synthesized

A

you synthesize them at the cell body, at the nucleus where the DNA and ribosomes are. Usually larger precursor peptides that are cleaved to smaller transmitters

21
Q

mu receptors are preferentially activated by

A

endorphins and selectively activated by endorphins

22
Q

delta receptor preferentially activated by

A

enkephalins and endorphins

23
Q

kappa receptor preferentially activated by

A

dynorphins

24
Q

Three ways opioids inhibit neural activity

A
  1. post synaptic inhibition - receptors activate a G protein that opens k+ channels. hypolarized.
  2. axoaxonic inhibition - heteroreceptors (presynaptic)- activate G proteins that close Ca2+ channels, reducing transmitter release.
  3. Presynaptic autoreceptors - reduce release of co-localized NT.
25
Q

all opioid receptors are coupled to ____ that inhibit ______

A

GI proteins, adenylyl cyclase-cAMP

26
Q

Partial agonist of opium

A

buprenorphine

27
Q
pure antagonists (2) of opium 
have high \_\_\_\_, low \_\_\_\_ for receptors
A

naloxone, naltrexone

high affinity, low efficacy

28
Q

what do endogenous opioids and opioids do in relation to pain when they bind receptors

A

inhibit pain signal transduction at multiple sites

29
Q

spinal cord (spinal analgesia)

A

opioid interneurons can inhibit. pain projection neurons
do so by activating descending pathways from brain to spine either by
1. inhibit pain projection neurons
2. inhibit excitatory interneurons that synapse on pain projection neurons

30
Q

opioids activate two descending pain-inhibiting pathways originating in the ___

A

PAG

31
Q

what do opioid projections from PAG do

A

disinhibit raphe (5HT) and locus coeruleus (NE) descending projections that suppress pain signals in the spinal cord

32
Q

what do low doses of opioids provide

A

pain relief, constricted pupils, drowsiness, inability to concentrate, dreamy sleep

33
Q

what do high doses of opioids provide

A

abnormal state of elation or euphoria

34
Q

what do highest doses of opioids cause

A

unconsciousness and death which happens due to suppression of brainstems respiratory centre

35
Q

how do we therapeutically administer opioids

A

intra-muscularly, orally (slow absorption not as euphoric)

36
Q

how do we recreationally administer opioids

A

more rapid means such as inhalation, snorting, sub-cutaneous, IV

37
Q

Aversive effects of opioids (4)

A

dysphoria, anxiety, nausea, restlessness

reduced GI motility hence constiption

38
Q

IV administration of opioids lead to which risks

A

infection
collapsed veins
liver/kidney damage

39
Q

opioids activate ________ and this contributes to

A

mesolimbic DA pathway, opioid reinforcement

40
Q

Mu-receptor activation does what in relation to DA

A

inhibit GABA neurons in VTA, which disinhibit DA neuron firing, increasing DA release

41
Q

Tolerance of which effects develop quickly, and which develop more slowly

A

analgesia/pleasurable tolerance = quick

constipation/pupilary dilation = slow

42
Q

withdrawal of opioid drugs symptoms

A

depress CNS function, rebound hyperactivity.

43
Q

opioid antagonist can

A

precipitate withdrawal symptoms

44
Q

opioid antagonist in _____ or _____ trigger physical withdrawal

A

Locus coeruleus or PAG

45
Q

opioid antagonist in _____ or _____ trigger aversive emotional effects withdrawal

A

NAc and Amygdala

46
Q

Methadone is what

A

opioid agonist, taken orally can help prevent severe withdrawal symptoms