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Pharm Exam 2 > Opioid Agonists > Flashcards

Opioid Agonists Flashcards

1
Q

MOA of opioids

A

increase K conductance, inhibition of ca channels, decreased neurotransmission, and pain modulators

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2
Q

location of opioid receptors

A

BRAIN: PAG, RVM, locus ceruleus, and hypothalamus; SPINAL CORD: substantia gelatinosa (L2+3); OUTSIDE CNS: sensory neurons and immune cells

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3
Q

Direct application of opioids to the dorsal horn (substantia gelatinosa) causes? what is usually given

A

intense analgesia; LA + opioid

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4
Q

example of administration of opioid to pain receptors outside the cns

A

intraarticular morphine

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5
Q

name the mu 1 agonists

A

morphine, endorphins, synthetic opioids

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6
Q

name the mu 2 agonists

A

endorphins, morphine, sythetic opioids

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7
Q

name the kappa agonists

A

Dynorphins

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8
Q

name the delta agonists

A

Enkephalins

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9
Q

what drugs antagonize mu1, mu2, kappa, and delta receptors?

A

naltrexone, naloxone, and nalmefene

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10
Q

list the effects of mu1 receptor agonism

A

supraspinal and spinal analgesia, euphoria, low abuse potential, miosis, bradycardia, hypothermia, and urinary retention

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11
Q

list the effects of mu2 receptor agonism

A

spinal analgesia, depression of ventilation, physical dependence, marked constipation

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12
Q

list the effects of kappa receptor agonism

A

spinal and supraspinal analgesia, dysphoria, and sedation, low abuse potential, miosis, diuresis

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13
Q

list the effects of delta receptor agonism

A

spinal and supraspinal analgesia, depression of ventilation, physical dependence, minimal constipation, urinary retention

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14
Q

list the cv effects of opioids

A

decreased sns tone in peripheral veins causing decrease in vr, co, and bp; ortho hypo and syncope

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15
Q

one potential cardiac benefit of opioids

A

cardioprotective; may help prevent MIs

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16
Q

list pulm effects of opioids

A

decreased responsiveness of ventilation centers to co2; increases paco2 causing a shift to the right

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17
Q

what is the drug of choice to antagonize ventilatory depression? how does it work and what other benefit does it have

A

physostigmine; increases cns levels of ach; does not antagonize analgesic effect

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18
Q

mu2 and kappa receptors cause this; which would eventually lead to __________ in opioid OD

A

respiratory depression; apnea, miosis, hypoventilation, coma

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19
Q

list the cns effects of opioids

A

decreased cbf and possibly icp; myoclonus with large doses; chest wall and abdominal muscle rigidity

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20
Q

treatment of chest wall and abdominal rigidity associated with opioids

A

muscle relaxant or naloxone

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21
Q

caution with opioids in head injuries because

A

decreased wakefulness, miosis, paco2

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22
Q

list gi effects of opioids

A

sphincter of oddi spasms (spasm of biliary smooth muscle); delayed gastric emptying and constipation; n/v

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23
Q

least drugs from most likely to least likely to cause oddi spasms

A

fentanyl, morphine, meperidine

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24
Q

least treatment drugs for oddi spasms

A

glucagon, naloxone, atropine, nalbuphine, ntg

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25
Q

most common gu s/e of opiods

A

urinary urgency

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26
Q

cutaneous effects of opioids

A

flushing d/t histamine release in face, neck, and chest

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27
Q

how long does it typically take tolerance to develop

A

2-3 weeks

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28
Q

how long does it typically take morphine tolerance to build up

A

25 days

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29
Q

downregulation occurs when

A

opioid receptors become desensitized by reduced transcription and subsequently have a reduced number of receptors

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30
Q

meperidine and fentanyl onset of withdrawals; peak intensity; duration

A

2-6 hours; 6-12 hours; 4-5 days

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31
Q

morphine and heroin onset of withdrawals; peak intensity; duration

A

6-18 hours; 36-72 hours; 7-10 days

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32
Q

methadone onset of withdrawals; peak intensity; duration

A

24-48 hours; 3-21 days; 6-7 weeks

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33
Q

morphine onset, peak, and duration

A

onset 15-30 minutes; peak ivp 30-35 mins; peak im 45-90 mins; duration 4-5 hours

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34
Q

PO morphine first pass

A

25%

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35
Q

morphine accumulates rapidly in the

A

kidneys, liver, and skeletal muscle

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36
Q

gold standard opioid

A

morphine

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37
Q

morphine effects which kind of fibers the most

A

c fibers

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38
Q

what kind of pain is morphine good for

A

dull, visceral, skeletal muscle, or joint pain; intermittent pain

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39
Q

morphine metabolites

A

morphine 3 glucoronide (inactive); morphine 6 glucoronide (active)

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40
Q

how is morphine metabolized

A

glucoronic acid conjugation in hepatic and extrahepatic sites

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41
Q

with renal patients, we worry about giving them morphine because

A

they can have prolonged respiratory depression

42
Q

morphine has an increased e 1/2 time because

A

of active metabolite morphine 3 glucoronide

43
Q

morphine has a higher analgesic potency and slower offset in

A

women

44
Q

meperidine is an agonist at

A

mu, kappa, a2 opioid receptors

45
Q

list the analogues of meperidine

A

the fentanyls: fentanyl, alfentanil, sufentanil, remifentanil

46
Q

meperidines have similar structures to

A

lidocaine and atropine

47
Q

duration of meperidine

A

2 to 4 hours

48
Q

hepatic first pass of meperidine

A

80%

49
Q

metabolism of meperidine

A

hepatic

50
Q

what percent of meperidine is protein bound

A

60%

51
Q

elimination of meperidine

A

kidneys

52
Q

e 1/2 time of meperidine

A

3-5 hours

53
Q

with renal failure e 1/2 time of meperidine may be

A

35 hours

54
Q

meperdine toxicity

A

delirium, myoclonus, seizures

55
Q

uses for meperidine

A

post op shivering, intrathecal, post op analgesia

56
Q

besides meperidine, what else might we use for post op shivering

A

clonidine

57
Q

fentanyl is ___x more potent than morphine

A

75-125 x

58
Q

peak time of fent in the brain

A

6.4 mins

59
Q

lung first pass of fent

A

75%

60
Q

fent is metabolized by

A

cyp3a

61
Q

principal metabolite of fent

A

norfentanyl

62
Q

excretion of fentanyl

A

kidneys

63
Q

do we need to alter the dose of fent for elderly or liver patients

A

no

64
Q

compared to the other meperidine derivatives, fentanyl’s context sensitive half time is

A

much much higher

65
Q

when giving fent to someone on bypass, we worry about

A

not enough fent getting to blood - it sticks to the machine

66
Q

fentanyl uses

A

solo surgical anesthesia, intrathecal. transmucosal. transdermal

67
Q

1 mg of PO fentanyl is equivalent to

A

5 mg iV morphine

68
Q

cv effects of opioids

A

depressed carotid sinus baroreceptor reflex causing bradycardia, decreased bp and CO

69
Q

most prominent s/e of fent

A

sz like activity, modest increase in icp

70
Q

sufentanil is __x more potent han fentanyl

A

5-12x

71
Q

sufentanil is 92.5% bound to

A

alpha 1 acid glycoprotein

72
Q

excretion of sufentanil

A

renal and fecal

73
Q

main s/e of sufentanil

A

chest wall and abdominal muscle rigidity; bradycardia leading to decreased CO

74
Q

alfentanil is ___ less potent than fentanyl

A

1/5th less

75
Q

alfentanil 1/2 time is prolonged in these patients

A

cirrhosis

76
Q

alfentanil is high protein bound

A

no right answer, just a reminder - like sufentanil

77
Q

metabolite of alfentanil

A

noralfentanil

78
Q

what drug has a quicker onset than fentanyl and sufentanil

A

alfentanil

79
Q

remi is dosed by

A

ibw

80
Q

remi has a quick peak effect at

A

1.1 min

81
Q

remi + prop will cause

A

synergistic depression of ventilation

82
Q

clearance of remi is faster than

A

alfentanil

83
Q

plasma steady state of remi is

A

10 mins

84
Q

remi is excretion is unaffected by

A

renal or hepatic disease

85
Q

e 1/2 of remi

A

6.3 mins

86
Q

remi is not recommended for

A

spinal or epidurals

87
Q

before stopping remi, you should consider

A

longer acting opioid or supplementation with multimodal

88
Q

main s/e of remi

A

sz like activity, n/v, depression of ventilation, decreased bp and hr, hyperalgesia from previous exposure to large opioid doses and tolerance

89
Q

hydromorphone is _x more potent than morphine

A

5

90
Q

redose dilaudid q

A

4 hours

91
Q

uses, s/e, and metabolites are the same as

A

morphine

92
Q

unlike morphine these drugs do not release histamine

A

fent and dilaudid

93
Q

codeine can be given

A

PO or IM

94
Q

codeine e 1/2 time

A

3-3.5 hours

95
Q

codeine metabolism

A

liver

96
Q

120 mgs of codeine equals

A

10 mgs of morphine

97
Q

main s/e of codeine

A

physical dependence, minimal sedation, n/v, constipation, dizziness

98
Q

tramadol is less potent than morphine by

A

5-10x

99
Q

tramadol mostly affects which receptors

A

mu

100
Q

worrisome tramadol interaction

A

warfarin

101
Q

unlike fentanyl, ____ does not build up in tissues

A

remi

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