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Drugs and Behavior > Exam 3: Opiates > Flashcards

Exam 3: Opiates Flashcards

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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
heroin ROA
nasal, inhalation, injection "skin-popping": subcutaneous injection "mainlining": IV injection - usually later in addiction
26
Absorption of heroin
low bioavailability if takn orally - first pass metabolism rapid when injected/snorted
27
distribution heroin
heroin 10x more lipid soluble than morphine - faster actions passes BBB and placental barrier
28
metabolism and elimination heroin
broken in liver into active metabolites: morphine and morphine-6-glucuronide elimination: urine
29
morphine ROA
intra-muscular injection (hospital setting), oral
30
absorption and distribution of morphine
absorption: low bioavailability oral (25%) distribution: crosses brain slower than heroin - less lipid soluble
31
metabolism and excretion morphine
active metabolite: morphine-6-glucuronide - gets into brain quicker than morphine - 10x more potent than morphine elimination: urine
32
fentanyl ROA
injection, transdermal patch, oral, intranasal
33
absorption fentanyl
highest bioavailability is injection intranasal and transdermal patch lower with oral
34
distribution fentanyl
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
35
metabolism and elimination of fentanyl
metabolism: brokwn down in liver into inactive norfentanyl elimination: urine
36
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
B-endorphins
37
thalamus, striatum, PAG, spinal cord
enkephalins
38
striatum, hippocampus, hypothalamus, nucleus accumbens
dynorphins
39
endogenous opioid peptides
B-endorphin, enkephalins, dynorphins
40
opioids frequently co-expressed with other neurotransmitters
- GABA in striatum | - GABA and glutamate in spinal cord
41
effects of opiates mediated by what 3 receptor types
Mu, Delta, Kappa
42
where are opioid receptors distributed?
CNS: cortex, limbic system, basal ganglia, spinal cord, enteric nervous system
43
endogenous peptide of mu receptors
endorphin
44
where are mu receptors for analgesia
medial thalamus, PAG, median raphe, spinal cord
45
where are mu receptors for feeding and positive reinforcement
nucleus accumbens and hypothalamus
46
where are mu receptors for mood
amygdala
47
where are mu receptors for cardiovascular and respiratory depression, cough control, nausea
brainstem - medulla
48
where are mu receptors for sensory integration
thalamus, striatum
49
where are delta receptors most commonly found and then other location
forebrain | cerebral cortex, thalamus, striatum, spinal cord
50
endogenous peptides of delta receptors
endorphin and enkephalin
51
role of delta receptors
modulate olfaction, motor integration, reinforcement, cognitive function learning, memory, attention
52
overlap of mu and delta receptors suggest
modulation of both spinal and supraspinal analgesia
53
major peptide of kappa receptors
dynorphin
54
where are kappa receptors found
striatum, hippocampus, amygdala, hypothalamus, and pituitary
55
what do kappa receptors have a role in
regulation of pain perception, gut motility, dysphoria make you feel bad when they are activated
56
effects of heroin, morphine, methadone at mu receptor
agonists
57
effects of buprenorphine at mu receptor
partial agonist
58
effects of naltrexone and narcan at mu receptors
antagonists
59
3 ways opioids inhibits nerve activity
postsynaptic inhibition axoaxonic inhibition presynaptic autoreceptors
60
all opioid receptors are
inhibitory and metabotropic
61
postsynaptic inhibition
receptors activate a G protein that opens K+ channels so K+ leaves cell, hyperpolarizing postsynaptic cells reducing the firing rate
62
axoaxonic inhibition
receptors activate G protein that close Ca channels, reducing release of neurotransmitter in this case an opioid is inhibiting a different presynaptic neuron
63
presynaptic autoreceptors
activate G proteins and reduce release of co-localized neurotransmitter limiting the same presynaptic neuron
64
how to get reinforcing aspects of opioids
B-endorphin and opioid drugs inc VTA cell firing by inhibiting the inhibitory GABA cells which disinhibits and turns on DA
65
effects of dynorphin on mesolimbic dopamine
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
chronic use of opiates leads to
neuroadaptive changes, responsible for tolerance, sensitization, and dependence
67
tolerance and opioids
- 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
opioid overdose
-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
what are the opiate user's desired effects?
analgesia cough suppression sedation - to help sleep euphoria
70
Mu1
analgesia and euphoria
71
Mu2
constipation, respiratory depression
72
Kappa
spinal analgesia, dysphoria
73
delta
analgesia through endorphin, enkephalin, dynorphin system | also dysphoria
74
2 pain pathways mediated by mu
ascending pathway: from periphery to brain - tells us we are hurt descending pathway: PAG - shuts down the ascending pathway to stop pain
75
how do opioids effect pain pathway
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
affective component of pain - emotional pain is regulated by what
anterior cingulate cortex
77
common symptoms of opiate intoxication
- miosis: pin point pupils - nodding - hypotension - depressed respiration - bradycardia - euphoria - floating feeling
78
acute effects of opiates
euphoria, drowsiness, body warmth, heavy feeling in limbs, dec sex drive, impaired social interactions
79
physiological effects of opioid use
respiratory depression lowered core body T, flushed skin itching - release of histamine pupillary constriction - pin point
80
long term effects of opioid use
``` impotence - sexual dysfunction constipation-people take imodium when do not have access to opiates -hypoxia -collapsed veins -dec immune function ```
81
what do people tale when do not have access to opiates, it is for constipation
imodium
82
opioid withdrawal results in
rebound hyperactivity - opposite symptoms of opioid use
83
fentanyl and withdrawal
symptoms 4-6hrs after last use peak 12 hrs post use last 5 days
84
morphine/heroin and withdrawal
symptoms 6-18 hours after last use peak 36-72 hrs post use last 7-10 days
85
methadone and withdrawal
symptoms 24-48 hrs after last use peak 3-21 days post use last 6-7 WEEKS

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