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High Yield Apex Cards For Boards > Opioids > Flashcards

Opioids Flashcards

1
Q

Tranduction

A

stimulus > AP

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2
Q

Transmission

A

signal from peripheral to central viaa 3 neuron system

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3
Q

describe the 3 order neuron system that makes up transmission

A

1st order: periphery to dorsal root ganglion in dorsal horn

2nd Order: dorsal horn to thalamus

3rd order: Thalamus to cerebral cortex

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4
Q

Modulation

A

signal modified as it advances up to cerebral cortex

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5
Q

where does perception occur?

A

occurs in cerebral cortex and limbic system

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6
Q

what is the most important site of pain signal modulation?

A

substania gelationosa in dorsal horn (rexed lamina 2&3)

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7
Q

outline the descending inhibitory pathway. What part of pain process is this?

A

part of modulation

periaquaductal gray > substania gelatinosa

rostroventral medulla > substania gelatinosa

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8
Q

when is pain inhibited? what step of pain process would this fall under?

A

modulation

  1. spinal neurons release GABA and or Glycine
  2. descending pain pathway releases NE, serotonin, and endorphins
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9
Q

pain is augmented by what?

A

central sensitization
wind up

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10
Q

what drugs target tranduction?

A

NSAIDs
LAs
steroids
antihistamines
opioids

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11
Q

what drugs target transmission?

A

LAs

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12
Q

what drugs target modulation

A

neuraxial opioids
NMDA antagonists
alpha 2 agonists
AchE Inhibitors
SSRIs
SNRIs

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13
Q

what drugs target perception?

A

general anesthetics
opioids
alpha 2 agonists

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14
Q

describe opioids mechanism of action

A
  1. opioid binds receptor
  2. G protein activated
  3. adenylate cyclase inhibited
  4. decreased cAMP production
  5. decreased Ca++ condcutance into cell > decreased neurotransmitter release from pre-synaptic cell
    6.^ K+ conductance out of cell > hyper polarizes post synaptic membrane.
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15
Q

name the opioids receptors

A

Mu
delta
kappa
ORL-1

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16
Q

Where are opioid receptors located?

A

Brain
spinal cord
peripheral

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17
Q

Where are opioid receptors located in the brain specifically?

A

periaquductal gray, locus coeruleus, rostral ventral medulla

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18
Q

Where are opioid receptors located in the spinal cord specifically?

A

primary afferant neurons in dorsal horn and interneurons

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19
Q

Where are opioid receptors located in the periphery specifically?

A

sensory neurons and immune cells

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20
Q

Mu opiod receptor effects

A

bradycardia
miosis
urinary retention
N/V
prurits
sedation
euphoria

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21
Q

what are the effects of delta opiod receptor

A

urinary retention
prurits

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22
Q

what are the affects of kappa opiod receptor

A

diuresis
anti-shivering
miosis
sedation/dysphoria
hallucinations/delerium

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23
Q

what effects to all opiod receptors have in common?

A

supraspinal and spinal analgesia
resp depression

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24
Q

specific effects of Mu1 receptor

A

analgesia spinal and supraspinal
bradycardia

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25
Q

specific effects of Mu2 receptor

A

spinal analgesia
bradycardia
resp depression
constipation
physical dependence

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26
Q

specific effects of Mu3 receptor

A

immune supression

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27
Q

how are opioids metabolised? what is the exception?

A

hepatic biotransformation

exception is Remi through non-specific esterases

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28
Q

which opioids have active metabolites?

A

morphine
meperedine
hydromorphone (some texts say yes some say no)

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29
Q

morphine active metabolites and which are active vs inactive?

A

morphine-3-glucuronide - inactive
morphine-6-glucuronide - active

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30
Q

tell me about M-6-G

A

water soluble so tends not to cross BBB at normal concentrations.

risk of accumlation in renal failure though and then some can cross BBB

there is also risk of this if you give healthy person lots of morphine I beleive

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31
Q

meperidine active metabolite

A

normeperidine

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32
Q

tell me about normeperidien

A

1/2 as potent as meperidine
decreases seizure threshold and increases CNS excitability
avoid in dialysis patient and caution in the elderly

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33
Q

hydromorphone active metabolite and how is it excteted?

A

hydromorphone-6-glucuronide
excreted by the kidneys

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34
Q

what happens when opioids stimualte the edinger westphal nucleus?

A

increased PNS stimulation of ciliary ganglion and Cranial nerve 3 > pupil constriction

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35
Q

does tolerance to pupil constriction from opiods occur?

A

no

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36
Q

how do opioids affect SSEP?

A

minimally, thus okay to use remi in spines

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37
Q

cv effects of opioids

A

brady cardia with minimal effects on BP in healthy patients

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38
Q

do opioids cause myocardial depression?

A

No, only when they are combined with nitrous oxide

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39
Q

billiary effects of opioids. Which opiod does it the least?

A

contraction of sphincter of oddi > increased biliary pressure.

meperidine does this the least

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40
Q

are there gendener differences in opiods effects?

A

yes

in women:
greater analgesic potency
slower onset
^ DOA
lower post-op opioid consumption

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41
Q

name the naturally occurring opioids and from where they are derived

A

phenanthrene derivatives
morphine
codeine

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42
Q

name the semi-synthetic opioids and from where they are derived

A

morphine derivatives:
hydromorphone
heroin
naloxone
naltrexone

thebaine derivatives:
oxycodone

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43
Q

name the systhetic opioids and their respective class

A

piperdines: meperidine

phenylpiperdines:
fentanyl
sufentanil
remifentanil
alfentanil

diphenylpropylamines: methadone

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44
Q

decribe the opoids and their relative potency

A

meperidine 100mg
morphine 10mg
dialudid 1.4mg
alfentanil 1000mcg
remi 100mcg
fentanyl 100mcg
sufentanil 10mcg

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45
Q

the potency of methadone depends on what?

A

patients daily opioid therapy and the duration of therapy

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46
Q

define dependence

A

will go through withdrawal if they stop drug

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47
Q

define addiction

A

can’t stop using it despite negative consequences

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48
Q

tolerance and physical dependence are most likely due to what?

A

receptor desensitization and increased sythesis of cAMP

49
Q

two what two physical affects of opiods does tolerance not develop?

A

miosis and constipation

50
Q

early s/s of opioid withrawal?

A

diaphoresis, insomnia, restlesness

51
Q

late s/s of opioid withdrawl?

A

abdominal cramping and N/V

52
Q

which opiodis release histamine?

A

meperidine
morphine
codeine

53
Q

meperidine mech of action

A

stimulates Mu and kappa receptors
also weak SSRI

54
Q

which opioid is structurally similar to atropine? what can this cause?

A

meperidine
anticholinergic side effects

55
Q

what does normeperidine do?

A

can cause myoclonus
decrease seizure threshold and increase CNS excitability

56
Q

when to avoid meperidine

A

in dialysis pt and elderly

57
Q

when can meperidine cause serotonin syndrome?

A

if patient is taking MAOIs

58
Q

s/s of serotonin syndrome

A

hyperthermia
mental satus changes
hypereflexia
seizures
death

59
Q

name some MAOIs

A

phenelzine
isocarboxazid
tranylcypromine

60
Q

which opioid has the lowest pKA? what is it?

A

alfentanil at 6.5

61
Q

what is the significance of the low pKA of alfentanil?

A

90% ionized at physiolgic pH so very fast onset

62
Q

what is alfentanil useful for?

A

blunt hemodynamic response to short very stimulating procedures like:
intubation and retrobulbar block

63
Q

how is alfentanil metabolised?

A

CYP3A4 metabolism but with a low hepatic extraction rate

64
Q

what is the significance of alfentanils low hepatic extraction rate?

A

can be prolonged by erythromycin

65
Q

remifentanil mech of action

A

mu r agonist

66
Q

remi’s context sensitive half time?

67
Q

in what route can you not use remi? why?

A

neuraxial because it has glycine

68
Q

remi dose

A

0.1-1.0mcg/kg/min

69
Q

remi dose is based on what weight? why?

A

lean body weight beacause it does not distribute throughout body becaue it is metabolized so quickly

70
Q

what drugs can prevent OIH from remifentanil?

A

ketamine and magnesium sulfate

71
Q

which opiod is a racemic mixture?

72
Q

good uses for methadone?

A

chronic tx or opioid abuse
chronic pain syndromes
cancer pain

73
Q

methadone mech of action

A

mu agonist and NMDA antagonist
inhibits reuptake of monoamines in synaptic cleft

74
Q

methadone oral bioavailability

75
Q

methadone DOA

76
Q

which opioid has risk of prolonging QT syndrome

77
Q

oliceridine mech of action

A

mu agonist

78
Q

when oliceridine indicated

A

chronic pain when other opioids fail

79
Q

daily dose of oliceridine should not exceed

80
Q

when to changes oliceridine dose

A

not for renal or mild-mod hepatic failure

do decrease dose when pt is on CYP3A4/CYP2D6 inhibitors

81
Q

oliceridine contraindications

A

gi obstruction including paralytic ileus

82
Q

oliceridine SE

A

mild QT prolongation
^ risk of seizures in pt with history of seizures

83
Q

skeletal muscle ridigity is most common from which opioids?

A

lipphilic opioids
sufentanil, fentanyl, femifentanil, alfentanil

84
Q

how is opioid induced s. muscle rigidity cuased?

A

from rapid IV administration

85
Q

where is the greatest resitance to ventilation during opioid induce s. muscle rigidity?

86
Q

tx for opioid induced skeletal m. rigidity

A

paralysis and intubation

87
Q

pro/cons of partial opioid agnoists

A

analgesia with decreased risk of resp depression

low risk of dependence

ceiling effect

88
Q

name some partial opioid agonists

A

buprenorphine
nalbuphine
butorphanol

89
Q

buprenorphine mech of action

A

partial mu agonist

90
Q

bupreorphine analgesia compared to morphine

91
Q

buprenorphine reversability with naloxone?

A

hard to reverse because it has such great affinity for Mu receptor

92
Q

buprenorphine DOA

93
Q

other admin route available for buprenorphine

A

transdermal

94
Q

nalbuphine mech of action

A

kappa agonist
mu antagonist

95
Q

nalbuphine analgesia compared to morphine

A

about the same

96
Q

nalbuphine reversability with naloxone

A

yes, reversible

97
Q

nalbuphine effects on CV system?

A

no increase in BP, HR, PAP, RAP, so useful in pt with history of heart disease

98
Q

butorphanol mech of action

A

kappa agonist
mu antagonist

99
Q

butorphanol analgesia compared to morphine

100
Q

can butorphanol be reversed by naloxone?

101
Q

what is anothre use of butorphanol?

A

post-op shivering

102
Q

name other partial opioid agonists

A

pentzocine
nalorphine
bremazocine
dezocine
meppazinol

103
Q

name some opioid antagonist

A

naloxone
methylnaltrexone
nalmefene
naltrexone

104
Q

naloxone mech of action

A

competitively antagonize mu, kappa, delta receptors but greatest affinty for mu r

105
Q

naloxone dose

A

1-4mcg/kg but better to just give 20-40mcg at a time to prevent overshooting

106
Q

naloxone doa

A

30-45min so may need re-dose

107
Q

can you use naloxone in a gtt?

108
Q

biggest risk with naloxone?

A

in a patient with pain it can cause sympathetic stimulation > neurogenic pul edema, tachycardia, dysrhthmias and sudden death

109
Q

does naloxone cross the placenta?

A

yes, so it can precipitate opioid withdrawal in neonate

110
Q

beside resp depression, what else might you want to reverse with naloxone?

A

opioid induced pruritis

111
Q

does methylnaltrexone cross the BBB?

112
Q

tell me more about methylnaltrexone

A

can reverse opioid induce resp depression

useful to mitigate peripheral risks of opioids like opioid induce bowel dysfunction

113
Q

tell me about nalmefene

A

like naloxone but doa is much longer
can be used to maintain recovering opioid abusers

114
Q

tell me about naltrexone

A

does not undergo signficant 1st pass metaboilsm
only given orally
doa 24hrs
extended release can be used for etoh withdrawal and also to maintain recovering opioid abusers

115
Q

what is the gold standard for post op opioid delivery?

116
Q

was does PCA basal rate do and not do?

A

does increase risk of resp depression

does not provide sup pain releif or improve sleep

117
Q

resp depression is RR < ?

118
Q

what is the lockout time on PCA pump based on?

A

time for demand dose to reach an effective plasma concentration

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