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Pharm Exam 2 > Opioid Agonists > Flashcards

Opioid Agonists Flashcards

(101 cards)

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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
most common gu s/e of opiods
urinary urgency
26
cutaneous effects of opioids
flushing d/t histamine release in face, neck, and chest
27
how long does it typically take tolerance to develop
2-3 weeks
28
how long does it typically take morphine tolerance to build up
25 days
29
downregulation occurs when
opioid receptors become desensitized by reduced transcription and subsequently have a reduced number of receptors
30
meperidine and fentanyl onset of withdrawals; peak intensity; duration
2-6 hours; 6-12 hours; 4-5 days
31
morphine and heroin onset of withdrawals; peak intensity; duration
6-18 hours; 36-72 hours; 7-10 days
32
methadone onset of withdrawals; peak intensity; duration
24-48 hours; 3-21 days; 6-7 weeks
33
morphine onset, peak, and duration
onset 15-30 minutes; peak ivp 30-35 mins; peak im 45-90 mins; duration 4-5 hours
34
PO morphine first pass
25%
35
morphine accumulates rapidly in the
kidneys, liver, and skeletal muscle
36
gold standard opioid
morphine
37
morphine effects which kind of fibers the most
c fibers
38
what kind of pain is morphine good for
dull, visceral, skeletal muscle, or joint pain; intermittent pain
39
morphine metabolites
morphine 3 glucoronide (inactive); morphine 6 glucoronide (active)
40
how is morphine metabolized
glucoronic acid conjugation in hepatic and extrahepatic sites
41
with renal patients, we worry about giving them morphine because
they can have prolonged respiratory depression
42
morphine has an increased e 1/2 time because
of active metabolite morphine 3 glucoronide
43
morphine has a higher analgesic potency and slower offset in
women
44
meperidine is an agonist at
mu, kappa, a2 opioid receptors
45
list the analogues of meperidine
the fentanyls: fentanyl, alfentanil, sufentanil, remifentanil
46
meperidines have similar structures to
lidocaine and atropine
47
duration of meperidine
2 to 4 hours
48
hepatic first pass of meperidine
80%
49
metabolism of meperidine
hepatic
50
what percent of meperidine is protein bound
60%
51
elimination of meperidine
kidneys
52
e 1/2 time of meperidine
3-5 hours
53
with renal failure e 1/2 time of meperidine may be
35 hours
54
meperdine toxicity
delirium, myoclonus, seizures
55
uses for meperidine
post op shivering, intrathecal, post op analgesia
56
besides meperidine, what else might we use for post op shivering
clonidine
57
fentanyl is ___x more potent than morphine
75-125 x
58
peak time of fent in the brain
6.4 mins
59
lung first pass of fent
75%
60
fent is metabolized by
cyp3a
61
principal metabolite of fent
norfentanyl
62
excretion of fentanyl
kidneys
63
do we need to alter the dose of fent for elderly or liver patients
no
64
compared to the other meperidine derivatives, fentanyl's context sensitive half time is
much much higher
65
when giving fent to someone on bypass, we worry about
not enough fent getting to blood - it sticks to the machine
66
fentanyl uses
solo surgical anesthesia, intrathecal. transmucosal. transdermal
67
1 mg of PO fentanyl is equivalent to
5 mg iV morphine
68
cv effects of opioids
depressed carotid sinus baroreceptor reflex causing bradycardia, decreased bp and CO
69
most prominent s/e of fent
sz like activity, modest increase in icp
70
sufentanil is __x more potent han fentanyl
5-12x
71
sufentanil is 92.5% bound to
alpha 1 acid glycoprotein
72
excretion of sufentanil
renal and fecal
73
main s/e of sufentanil
chest wall and abdominal muscle rigidity; bradycardia leading to decreased CO
74
alfentanil is ___ less potent than fentanyl
1/5th less
75
alfentanil 1/2 time is prolonged in these patients
cirrhosis
76
alfentanil is high protein bound
no right answer, just a reminder - like sufentanil
77
metabolite of alfentanil
noralfentanil
78
what drug has a quicker onset than fentanyl and sufentanil
alfentanil
79
remi is dosed by
ibw
80
remi has a quick peak effect at
1.1 min
81
remi + prop will cause
synergistic depression of ventilation
82
clearance of remi is faster than
alfentanil
83
plasma steady state of remi is
10 mins
84
remi is excretion is unaffected by
renal or hepatic disease
85
e 1/2 of remi
6.3 mins
86
remi is not recommended for
spinal or epidurals
87
before stopping remi, you should consider
longer acting opioid or supplementation with multimodal
88
main s/e of remi
sz like activity, n/v, depression of ventilation, decreased bp and hr, hyperalgesia from previous exposure to large opioid doses and tolerance
89
hydromorphone is _x more potent than morphine
5
90
redose dilaudid q
4 hours
91
uses, s/e, and metabolites are the same as
morphine
92
unlike morphine these drugs do not release histamine
fent and dilaudid
93
codeine can be given
PO or IM
94
codeine e 1/2 time
3-3.5 hours
95
codeine metabolism
liver
96
120 mgs of codeine equals
10 mgs of morphine
97
main s/e of codeine
physical dependence, minimal sedation, n/v, constipation, dizziness
98
tramadol is less potent than morphine by
5-10x
99
tramadol mostly affects which receptors
mu
100
worrisome tramadol interaction
warfarin
101
unlike fentanyl, ____ does not build up in tissues
remi

Pharm Exam 2 (7 decks)

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