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Drugs and Behavior > Exam 3: Opiates > Flashcards

Exam 3: Opiates Flashcards

1
Q

dried powdered mixture of 20 alkaloids obtained from unripe seed capsules of the poppy
natural, harvested, contains psychoactive opiates

A

opium

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2
Q

any agent derived from opium

morphine, heroine

A

opiate

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3
Q

all substances (exogenous and endogenous) with morphine like properties

A

opioid

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4
Q

where is opium derived from

A

opium poppy: Papaver Somniferum
-originated in Asia/Middle east

harvest: only 10 days they produce this opium sac with opiates

sap can be directly or indirectly processed

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5
Q

2 primary psychoactive constituents of opium are

A

morphine and codeine

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6
Q

what does opium contain

A

morphine - main ingredient

codeine, thebaine, narcotine and other ingredients

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7
Q

3rd most popular ingredient of opium

A

thebaine: not used therapetically, causes convulsions

used to make oxycodone

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8
Q

narcotic analgesics

A

block pain

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9
Q

codeine

A

cough suppressant, not as much euphoria

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10
Q

heroin

A
  • made by adding 2 acetyl groups to morphine making it more lipid soluble
  • 10x more fat soluble - reaches brain faster
  • 3x more potent than morphine when injected
  • rapid action - dramatic euphoric effects
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11
Q

partial agonists

A

pentazocine (Talwin), nalbuphine (Nubain), and buprenorphine (Buprenex)

binds receptors with less potency than full agonists (morphine) but fewer side effects and less risk of dependence
-less anti pain and sedation

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12
Q

pure antagonists

A

naloxone and nalorphine
structurally similar but have no efficacy
- prevent or reverse effects of opioids

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13
Q

naloxone

A

administered in response to suspected opioid overdose (Narcan)

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14
Q

fully synthetic opioids

A

not derived from naturally occurring opioids

fentanyl and methadone

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15
Q

fentanyl

A

50x more potent than heroin
100x more potent than morphine
used for severe pain and cough, detoxification

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16
Q

methadone

A

long lasting
NMDA antagonist - blocks pain but you do not get a high
- helps opioid addiction - safe since not same abuse liability

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17
Q

5 types of semisynthetic narcotics

A 
krokodil 
heroin
hydromorphone (Dilaudid)
oxycodone (percodan)
buprenorphine (Buprenex)
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18
Q

6 types of totally synthetic narcotics

A 
Pentazocine (Tawin)
Meperidine (Demerol)
Fentanyl (sublimaze)
methadone (dolophine)
LAAM
propoxyphene (darvon)
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19
Q

which totally synthetc narcotic has a faster onset and shrter duration than morphine

A

meperidine (demerol)

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20
Q

schedule II opioids

A

fentanyl, hydrocodone, morphine, methadone, opium extract, thebaine

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21
Q

schedule I opioids

A

desomorphine, diacetylmorphine (heroin)

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22
Q

schedule III opioids

A

buprenorphine

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23
Q

schedule V opioids

A

codeine

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24
Q

opioids used in surgical intervention

A

buprenorphine

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25
Q

heroin ROA

A

nasal, inhalation, injection

“skin-popping”: subcutaneous injection

“mainlining”: IV injection - usually later in addiction

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26
Q

Absorption of heroin

A

low bioavailability if takn orally - first pass metabolism

rapid when injected/snorted

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27
Q

distribution heroin

A

heroin 10x more lipid soluble than morphine - faster actions

passes BBB and placental barrier

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28
Q

metabolism and elimination heroin

A

broken in liver into active metabolites:
morphine and morphine-6-glucuronide

elimination: urine

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29
Q

morphine ROA

A

intra-muscular injection (hospital setting), oral

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30
Q

absorption and distribution of morphine

A

absorption: low bioavailability oral (25%)
distribution: crosses brain slower than heroin - less lipid soluble

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31
Q

metabolism and excretion morphine

A

active metabolite: morphine-6-glucuronide

  • gets into brain quicker than morphine
  • 10x more potent than morphine

elimination: urine

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32
Q

fentanyl ROA

A

injection, transdermal patch, oral, intranasal

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33
Q

absorption fentanyl

A

highest bioavailability is injection intranasal and transdermal patch
lower with oral

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34
Q

distribution fentanyl

A

100x more potent than morphine - highly lipid soluble - more than heroin and morphine
rapid, widespread distribution to lungs, heart, kidneys, brain, liver, muscles

need less to get strong effects

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35
Q

metabolism and elimination of fentanyl

A

metabolism: brokwn down in liver into inactive norfentanyl
elimination: urine

36
Q

synthesized in POMC neurons of the arcuate nucleus and nucleus of solitary tract (NST)

-project to limbic system, brainstem, spinal cord, PAG, mesolimbic DA system

A

B-endorphins

37
Q

thalamus, striatum, PAG, spinal cord

A

enkephalins

38
Q

striatum, hippocampus, hypothalamus, nucleus accumbens

A

dynorphins

39
Q

endogenous opioid peptides

A

B-endorphin, enkephalins, dynorphins

40
Q

opioids frequently co-expressed with other neurotransmitters

A
  • GABA in striatum

- GABA and glutamate in spinal cord

41
Q

effects of opiates mediated by what 3 receptor types

A

Mu, Delta, Kappa

42
Q

where are opioid receptors distributed?

A

CNS: cortex, limbic system, basal ganglia, spinal cord, enteric nervous system

43
Q

endogenous peptide of mu receptors

A

endorphin

44
Q

where are mu receptors for analgesia

A

medial thalamus, PAG, median raphe, spinal cord

45
Q

where are mu receptors for feeding and positive reinforcement

A

nucleus accumbens and hypothalamus

46
Q

where are mu receptors for mood

A

amygdala

47
Q

where are mu receptors for cardiovascular and respiratory depression, cough control, nausea

A

brainstem - medulla

48
Q

where are mu receptors for sensory integration

A

thalamus, striatum

49
Q

where are delta receptors most commonly found and then other location

A

forebrain

cerebral cortex, thalamus, striatum, spinal cord

50
Q

endogenous peptides of delta receptors

A

endorphin and enkephalin

51
Q

role of delta receptors

A

modulate olfaction, motor integration, reinforcement, cognitive function
learning, memory, attention

52
Q

overlap of mu and delta receptors suggest

A

modulation of both spinal and supraspinal analgesia

53
Q

major peptide of kappa receptors

A

dynorphin

54
Q

where are kappa receptors found

A

striatum, hippocampus, amygdala, hypothalamus, and pituitary

55
Q

what do kappa receptors have a role in

A

regulation of pain perception, gut motility, dysphoria

make you feel bad when they are activated

56
Q

effects of heroin, morphine, methadone at mu receptor

A

agonists

57
Q

effects of buprenorphine at mu receptor

A

partial agonist

58
Q

effects of naltrexone and narcan at mu receptors

A

antagonists

59
Q

3 ways opioids inhibits nerve activity

A

postsynaptic inhibition
axoaxonic inhibition
presynaptic autoreceptors

60
Q

all opioid receptors are

A

inhibitory and metabotropic

61
Q

postsynaptic inhibition

A

receptors activate a G protein that opens K+ channels so K+ leaves cell, hyperpolarizing postsynaptic cells reducing the firing rate

62
Q

axoaxonic inhibition

A

receptors activate G protein that close Ca channels, reducing release of neurotransmitter
in this case an opioid is inhibiting a different presynaptic neuron

63
Q

presynaptic autoreceptors

A

activate G proteins and reduce release of co-localized neurotransmitter
limiting the same presynaptic neuron

64
Q

how to get reinforcing aspects of opioids

A

B-endorphin and opioid drugs inc VTA cell firing by inhibiting the inhibitory GABA cells which disinhibits and turns on DA

65
Q

effects of dynorphin on mesolimbic dopamine

A

it acts on kappa receptors on DA terminals and reduces release of DA causing dysphoria
it does this through axoaxonic synapses

when it binds it prevents VTA from releasing DA, get dysphoria associated with withdrawal symptoms

66
Q

chronic use of opiates leads to

A

neuroadaptive changes, responsible for tolerance, sensitization, and dependence

67
Q

tolerance and opioids

A
  • opioid receptor desensitization and internalization with chronic use
    • internalized so less receptor available
    • does not respond to natural levels of opioids, need more drug to get effects
  • compensation: upregulation of opioid receptors - body thinks receptor is broken so it makes more - this is problem when stop using opioids bc you have lots of receptors to bind transmitter and get huge sensitization
  • cross tolerance
68
Q

opioid overdose

A

-respiratory failure
-not all symptoms undergo tolerance at the same time (first euphoria goes away)
so people say lets take higher doses to get euphoria but you do not have tolerance to respiration yet, so when people take high doses it shuts down the ability to breathe - die

69
Q

what are the opiate user’s desired effects?

A

analgesia
cough suppression
sedation - to help sleep
euphoria

70
Q

Mu1

A

analgesia and euphoria

71
Q

Mu2

A

constipation, respiratory depression

72
Q

Kappa

A

spinal analgesia, dysphoria

73
Q

delta

A

analgesia through endorphin, enkephalin, dynorphin system

also dysphoria

74
Q

2 pain pathways mediated by mu

A

ascending pathway: from periphery to brain - tells us we are hurt

descending pathway: PAG
- shuts down the ascending pathway to stop pain

75
Q

how do opioids effect pain pathway

A

they inhibit the ascending pathway so brain does not get signal there is pain this is bc opioid receptors are in spinal cord

disinhibit (activate) descending pathway to stop pain

76
Q

affective component of pain - emotional pain is regulated by what

A

anterior cingulate cortex

77
Q

common symptoms of opiate intoxication

A
  • miosis: pin point pupils
  • nodding
  • hypotension
  • depressed respiration
  • bradycardia
  • euphoria
  • floating feeling
78
Q

acute effects of opiates

A

euphoria, drowsiness, body warmth, heavy feeling in limbs, dec sex drive, impaired social interactions

79
Q

physiological effects of opioid use

A

respiratory depression
lowered core body T, flushed skin
itching - release of histamine
pupillary constriction - pin point

80
Q

long term effects of opioid use

A 
impotence - sexual dysfunction
constipation-people take imodium when do not have access to opiates
-hypoxia
-collapsed veins
-dec immune function
81
Q

what do people tale when do not have access to opiates, it is for constipation

A

imodium

82
Q

opioid withdrawal results in

A

rebound hyperactivity - opposite symptoms of opioid use

83
Q

fentanyl and withdrawal

A

symptoms 4-6hrs after last use
peak 12 hrs post use
last 5 days

84
Q

morphine/heroin and withdrawal

A

symptoms 6-18 hours after last use
peak 36-72 hrs post use
last 7-10 days

85
Q

methadone and withdrawal

A

symptoms 24-48 hrs after last use
peak 3-21 days post use
last 6-7 WEEKS

Drugs and Behavior (27 decks)

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