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345A > Opioids: Nov 26th > Flashcards

Opioids: Nov 26th Flashcards

1
Q

where is opium derived from

A

Sap derived from the poppy (Papaver somniferum)

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2
Q

how long have the properties of opium been known for

A

1000s of years over the contents (hot climate where you can grow it

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3
Q

what is the difference between an analgesic and a narcotic

A 
analegisic= pain relief 
narcotic= opium based pain killers
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4
Q

anesthetics vs analgesics ?

A 
anes= knock out 
analgesic= alieviate pain
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5
Q

which is mj

A

analgesic

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6
Q

narcotic is a subcategory od opium

A

t

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7
Q

4 categories of opium

A

endogenous
alkaloids
semisynthetic
synthetic

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8
Q

example of a endogenous opium

A

endorphin (release to alleviate pain during physical endurance)

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9
Q

T: directly derived from sap

A

alkaloids

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10
Q

example of alkaloids 2

A

morphine and codeine (potency difference)

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11
Q

T: derivatives of directly extracted substance

A

semisyn

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12
Q

2 examples of semi

A

heroine (from codeine)

oxycodone (from morphine)

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13
Q

T: structurally different opiates (perfect molecule influence receptor)

A

synthetic

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14
Q

2 examples of synthetics

A

methadone and fentanyl

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15
Q

which class of drugs are opium

A

Exhibit euphoric (stimulant) and anxiolytic (depressant) effects, used as a medicine (anti-psychotic) NOT A HAL

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16
Q

which category of opiate has different subjective effects

A

derived= semisyn

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17
Q

since opium has no hallucinogenic properties we can rule what out

A

seretonin influence

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18
Q

different intake methods depend on what property of the drug

A

potency and resistance to metabolism

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19
Q

what effects do you have from oral opiod ingestion

A

mood alleviation (happy and relaxed), cough suppression (not coating throat)

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20
Q

what form of intake causes euphoria

A

inhalation

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21
Q

what are the 2 effects of intravenous

A

euphoria, pain relief

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22
Q

what happens to body temp and pupils

A

Decreased body temp (risk of hypothermia), pupil constriction (hal=widen opioids close to prep you for sleep)

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23
Q

how long does it take opioids to kick in when injected

A

2 min

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24
Q

why would anyone put themselves through injection

A

“rush” “flash”: intense euphoria = emotion within 2 min

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25
Q

other than euphoria what happens in stage 1 injection

A

Tingling/warmth in “lower abdomen” resembling sexual

orgasm = v reinforcing !!!

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26
Q

what is stage 2 after injection (2-3 hours after)

A

“on the nod”: tranquil drowsiness = soothed

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27
Q

what happens to sexual interest in stage 2

A

Reduction of sexual interest as a result of lowering testosterone levels

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28
Q

what is stage 3 after injection

A

withdrawal = SO RAPID

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29
Q

how does the injection cycle relate to poor outcomes for users

A

lower testosterone= low social dom and lack of interest in partner = isolation

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30
Q

T: street name China white, China girl, TNT, Apache, percopop

A

fentanyl (hit us before rest of world first)

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31
Q

trade name for fentanyl

A

Duragesic, Sublimaze around since the 70s

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32
Q

which opioids are which schedule

A

Schedule I = Heroin

Schedule II = Morphine, Methadone, Fentanyl Schedule V = Codeine, Oxycodone

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33
Q

3 ways fentynol is given

A 
Demerol – anaesthetic, “lollipop” – palliative care, Duragesic –
chronic pain (analgesia)
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34
Q

how does it compare to morphine in potency

A

100x (carfenanyl 1000x)

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35
Q

what is the fentaynol crisis

A

crisis of contamination

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36
Q

3 ways to intake fentanyl

A

oral, transdermal, insufflation

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37
Q

what is the problem and gain with fast fentanyl absorption

A

respiratory depression increases with faster

absorption but less nausea and itching

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38
Q

what makes fentanyl so effective

A

potent and resistant to metabolism

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39
Q

what is the synthetic opid used for sedation and analgesia

A

Desomorphine

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40
Q

why was desomo created

A

powerful surgical anesthetic back in 1930s (8x more potent than morhpine

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41
Q

what were the downside of desomorphines potency

A

Increase in respiratory depression, septicemia, and

cardiac arrest

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42
Q

what is septicaemia

A

arge amounts of bacteria are present in the blood from toxins in poop not going anywhere

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43
Q

how is crocodile related to desomorphine

A

synthesized version of desomorphine from codeine

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44
Q

3 street names for desomorphine synthesized from codeine

A

Krokodil, zombie, flesh-eating

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45
Q

krokodile has high toxicity from impure.. 2

A

preparation or reduction methods

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46
Q

2 things that are added to Kroc during preparation

A

paint thinner, HCL

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47
Q

what does the impure preparation cause 2

A

Inflammation liver, kidney

48
Q

3 this created during impure reduction method

A

gasoline/ kerosine, iodine. phosphorus

49
Q

3 things impure reduction methods cause

A

Thyroid damage, “Phossy Jaw”, gangrene

50
Q

T: a condition that occurs when body tissue dies

A

gangrene

51
Q

you can’t get addicted to Kroc due to terrible adverse effects

A

f such a powerful painkiller you don’t feel it until it wears off

52
Q

how is Kroc related to desomorphine

A

when someone tries to create desomorphine

53
Q

what is opium doing inside the body

A

agonizing the endogenous opiod system

54
Q

Proopiummelancortin, proenkephalin, prodynorphin what are these

A

endogenous opiod chemicals= free floating in bodies but bound to other things= under high duress enzyme cuts active portion out from rest of molecule

55
Q

T: separating the molecule into separate chains

A

cleavage

56
Q

what are the 2 steps to cleavage

A
  1. internal enzymatic action

2. active metabolite= morphine (cut morphine from molecule)

57
Q

Enzyme … converts codeine to morphine

A

CYP2D6 (responsible for endogenous functions as well)

58
Q

2 ways opium macts as a agoist

A
  1. cleavage

2. g protein metabotropic receptors

59
Q

what enzyme is responsible for cleavage

A

CYP2D6

60
Q

is the molecule after cleavage active

A

yes= double whammy!

61
Q

ipiods become G-protein bound to Metabotropic receptors- what does this mean

A

it changes the system- makes neurons return to resting potential sooner- they don’t fire

62
Q

how does opium return neurons to resting potential sooner

A

allowing k to influx inwards

63
Q

what is sensation vs perception

A

p: subjective interpretation of sensory signals
sensation: sensory experience

64
Q

how fast do neurons fire when you feel pain

A

fast

65
Q

how do opioids influence the system long term

A

makes neurons less likely to fire (depressant aspects)

66
Q

how can this explain runners high

A

produce endogenous endorphins so you can endure physical pain

67
Q

function of a pure agonist

A

pain relief

68
Q

2 pure agonists of the endoginist system

A

fentanyl and morphine (medical)

69
Q

function of partial agonism of endogenous system

A

Pain relief with no respiratory effect

70
Q

example of partial agonist

A

Buprenorphine (less potent)

71
Q

function of a mixed or agonist antagonist on endog system

A

Treating opioid addiction (occupy receptor s.o.a., block drug/other receptor)

72
Q

2 examples of mixed agonist antagonists

A

Naloxone, methadone (no high but dependance)

73
Q

why are they called mixed

A

they are agonizing receptors but they do nothing subjectively= antagonizing other chemicals e.g. the drug (implies how we use)

74
Q

the mixed antag/ agnostics are used as … in some countries

A

anxiolytic

75
Q

what are the 3 areas of pain perception you can target

A

periphery, CNS, protections from brain (proximal= brain/ distal= body)

76
Q

opioids agonism what?

A

endogenous opiod system

77
Q

how do opioids agonise the endo opiod system

A

by antagonizing the gABA (antagonist) system which stops endo opioids pain relief

78
Q

gaba supresses the inhibitory response of … receptors

A

dopamine = influx= reinforcing

79
Q

Suppression of the inhibitory response on dopamine receptors: where in brain does this happen

A

VTA

80
Q

what does opioids do in the Nucleus accumbans

A

Activation of u opioid receptors that inhibit the GABA neurons (inhibit GABA all over)

81
Q

as opium antagonists GABA what happens to dopamine

A

Allows dopamine to be released in VTA, and “enhancement” of the dopaminergic response

82
Q

what does the enhacement of the dopamine system do

A

motor and reward control

83
Q

ONE study in 1999 found relationship between opioids and reduce … receptor as a secondary function

A

glutamate = reason they don’t show excitement in response to down regulation of system 41:40

84
Q

what mechanism is acting in the body

A

inhibitory

85
Q

T: sensory pathways related to pain

perception

A

nociception

86
Q

T: in charge of sensory pain signal from receptor to spinal chord

A

Ad & C fibers

87
Q

what do opioids do at ad and c fibers

A

Inhibition of neurotransmission

88
Q

sensory pain signal

from spinal chord to Thalamus what NT involved 2

A

Glutamate & substance P

89
Q

what do opiods do to stop glutamate and substance p from sending pain signal to thalamus

A

Activation of medulla inhibits neurotransmission to thalamus

90
Q

2 ways to stop pain from getting to the brain?

2 ways to stop pain once in the brain?

A

slides 7-8=. 4 ways to stop pain in the body

91
Q

when pain meds targeting the PNS how is its effect on pain described

A

“dulling”/”blunting” of pain= take edge off

92
Q

how long until you see withdrawl with opioids

A

3-4 hours

93
Q

is there tolerance with opium

A

oh yes withdrawl tells you that

94
Q

is the tolerance rapid? dose dependant?

A

not rapid but dose dep

95
Q

what does it mean to say opiod tolerance is Accrued

A

the more you take the more tolerance

96
Q

what does it mean to say tolerance is relational

A

proportional to the amount you take

97
Q

opiod tolerance abides by allostatic principles what does this mean

A

system changes more permanently to adapt to enviro demands to try and achieve homeostasis

98
Q

opiod tolerance is selective to which properties 3

A

analgesia, euphoria, and respiratory depression

99
Q

how sensitive is opiod tolerance to conditioning effects

A

extremely= less of a dose in unfamiliar place= OD

100
Q

how long does withdrawl last

A

5-10 days ( can stretch out or take full hit now)

101
Q

what do you see in first 4-6 hours of withdrawl that intensifies at 3-4 day mark

A

craving = psycholigal

102
Q

when does the physioligcal aspect kick in and what is it

A

8-12 hours with flu symptoms =respritory and hyperthermia

103
Q

what is the third stage of withdrawl that kicks in at 48- 72 hours

A

secondary effects: pupil dilation (opposite of when on the drug), anorexia, piloerection (goosebumbs= cold turkey), spastic arm/leg movements (“kicking the habit”)

104
Q

does pupil dilation happen similarly in hallucinogens and opioids

A

f when on Hal when coming off opioids

105
Q

…% relapse after withdrawal associated with environment

A

90= evidence for conditioning

106
Q

why 90% relapse if not as dangerous as alc and barbiturates withdrawl

A

not dealing with psychological component causing relapse

107
Q

how long does LT vs short term detox last

A

LT 180 days

ST 30 days

108
Q

3 benefits to methadone and buprenorphine as detox

A

Prevent withdrawal, long-lasting effects, weak/no euphoria

109
Q

how well does methadone and bupren work for ST detox

A

moderate withdrawal for short-term

110
Q

what is the debate with using methadone clinics

A

Institutional control of addicts (i.e. not real treatment)

111
Q

how long is rapid vs ultra rapid detox

A 
rapid= 10 days 
ultra= 2 days
112
Q

can you go through rapid and ultra rapid awake

A

no induce coma

113
Q

T: binds as an agonist and induces opposite pharmacological response

A

inverse agonist (mixed agonist antag)= lowers response

114
Q

what inverse agonist is used in detox

A

naloxone

115
Q

how is buprenorphine different from methadone

A

does have analgesic properties= better for those who have been using for long time

116
Q

naloxone dereases withdrawal symptoms, decrease duration

A

f increases withdrawl

117
Q

Ultra-rapid in conjunction with …. for first few hours

A

sedation/anesthetized

345A (20 decks)

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