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Anes. Pharm. Me > Opioid and Opioid Antagonists > Flashcards

Opioid and Opioid Antagonists Flashcards

2
Q

What is a natural opioid and give example

A

Naturally derived from opiummorphine

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3
Q

What is a synthetic opioid and give example

A

Manufactured by synthesisfentanyl

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4
Q

What is a semisynthetic opioid and give example

A

Chemical modification of morphineherioin

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5
Q

What type of receptors do opioids bind?

A

G coupled protein receptors

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6
Q

Where in the body do opioids bind to receptors?

A

brain and spinal cord

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7
Q

What are the endogenous opioid ligands?

A

EnkephalinsEndorpinsDynorphins

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8
Q

How do opioids affect neurotransmitter release?

A

decrease

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9
Q

in the brain and spinal cord, where are opioid receptors?

A

Periaqueductal gray matteramygdalaCorpus striatumHypothalamusSpinal cord (substantia gelatinosa)

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10
Q

where is the mu1 receptor located?

A

supraspinal and spinal

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11
Q

What are the effects of the Mu1 receeptor?

A

Analgesia–main actionEuphoriaN/V, PruritisLow abuse potentialBradycardia

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12
Q

What binds to the Mu1 receptor?

A

Endorphins, morphine and sythetic opioids

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13
Q

Where is the Mu2 receptor?

A

spinal

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14
Q

What are the effects of the Mu2 receptor?

A

HypoventilationanalgesiaEuphoria, SedationPhysical dependenceConstipation

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15
Q

What binds to MU2 receptor?

A

Endorphins, morphine and sythetic opioids?

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16
Q

Where is the kappa receptor?

A

Supraspinal, spinal

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17
Q

What are the effects of the kappa receptor?

A

AnalgesiaRespiratory depressionDysphoriadiuresis

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18
Q

What binds to the kappa receptor?

A

DynorphinsAgonist-antagonist principallyNalbuphine

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19
Q

How is the kappa receptor in relation to high intensity pain?

A

resistant

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20
Q

Where are the delta opioid receptors?

A

supraspinal, spinal

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21
Q

What are the effects of the delta receptor?

A

AnalgesiaRespiratory depressionPhysical dependenceUrinary retention

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22
Q

What binds to delta receptors?

A

enkaphalins

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23
Q

Which receptors cause respiratory depression?

A

Mu2, Kappa, and delta

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24
Q

Which receptor would give you the feeling “I feel like I am going to die”?

A

Kappa

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25
Q

which receptor is associated with constipation?

A

Mu2

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26
Which receptors are associated with physical dependence?
Mu2 and Delta (kappa has low abuse potential)
27
what are the 4 classic side effects of neuraxial opioids?
PruritisN/VUrinary retentionVentilatory depression
28
Are neuraxial opioid specific or somatic or visceral pain?
visceral
29
What are the cardiovascular effects of most opioids?What is the exception?
decrease sympathetic tone and therefore decrease BP, HR. There are minimal effects on the contractilityMerperidine is the exception, it has anti muscarinic effects
30
How do opioids affect RR, Vt, MV, and PaCO2?
Decrease RR, INcrease Vt, but overall decreases MV, and thus increases PaCO2
31
What effect do opioids have on cough?
supress
32
What effects do opioids have on MAC?
reduce
33
What effects do opioids have on cerebral blood flow, metabolic rate and ICP?
Decrease CBF and CMRO2ICP increases due to increase PaCO2 from hypoventilation
34
Which opioid may cause siezures?
Merperidine, from accumulation of normerperidine
35
What is biliary colic?
Spasm of the sphincter of OddiFeels similar to anginaIf not relieved by NTG then it is biliary colic
36
What can you give to relieve pain associated with biliary colic?
nalaxone
37
How do you reverse biliary colic?
Glucagon 2mg IV
38
What are the GI side effects of Opioids?
N/Vconstipationdelayed gastric emptyingbiliary colic
39
Whar are the GU side effects of opioids?
Urinary retention due to increase in tone of ureter and vesicle sphincter
40
Which two opioids cause the most histamine release?
morphine and merperidine
41
what opioid side effect is associated with the Erdinger-Westphal nucleus?
Miosis--oculomotor nerve
42
What side effect of opioids is associated with difficulty to bag mask pt?
truncal rigidity
43
Which two effects of opioids aren't subject to tolerance?
Constipation and miosis
44
What are the triad of symptoms for an opioid overdose?
MiosisRespiratory depressionComa
45
What is the onset of morphine?
15-30 min onset with peak effect at 45-90 min
46
What is the peak effect of morphine?
45-90 min
47
What is the duration of morphine?
3-4 hours
48
How is morphine metabolized? What is the metabolite and how does it compare to morphine?
Metabolized via conjugation with glucuronic acid in liver and in kidney.Its metabolite is morphine-6-gucuronide, which is more potent than morphine
49
What is the dose for intraoperative analgesia of morphine?
.1/-1mg/kg
50
How does merperidine compare to morphine?
0.1 potency
51
How can merperidine be delivered?
IV, IM or PO?
52
How can morphine be delivered?
IV, IM
53
Wha tis the peak effect and duration time for merperidine?
Peak: 5-7 minDuration: 2-4 hours
54
How does merperidine behave like atropine/local?
blocks sodium channelcauses tachycardia, dry mouth, mydriasis
55
How is merperidine metabolized?
90% hepatic metabolism to normeperidine, which is renally eliminated
56
What is the dose of merperidine for post-op shivering?
12.5-25mg--1 time dose
57
how does fentanyl compare to morphine?
75-125 times more potent
58
Waht is the peak ffect and duration of fentanyl?
peak: 3-5 minutesduration 30-60 min
59
how can fentanyl be administered?
IV, transdermal, PO, intranasal
60
Fentanyl is _____ soluble and protein bound
lipid
61
Where is the first pass uptake of fentanyl?
lungs--up to 75%
62
HOw does sufentanil compare to fentanyl?
5-10x as potent with greater affinity for opioid receptor
63
what is the peak and duration of sufentanil?
Peak 3-5 minutes, duration 30-60 minutes
64
What is the dose for DL of sufentanil?
0.3-1mcg/kg 1-3 minutes before DL
65
What is the infusion rate for sufentanil?
0.5 mcg/kg followed by 0.5 mcg/kg/hr
66
How does alfentanyl compare to fentanyl?
1/10-1/5 as potent
67
What is the duration and peak of alfentanyl?
Peak 1.5-2 minutesDuration 10-20
68
HOw does renal failure affect Alfentanyl?
does not alter clearance
69
What are the uses for alfentanyl?
Because of its rapid on and off of intense analgesia, it is good for retrobulbar block or DL
70
What is the dose for alfentanyl?
5-10 mcg/kg
71
How does remifentanyl compare to fentanyl?
similar potency
72
What is the peak effect and duration of remifentanyl?
peak 1.5-2 minutesDuration 6-12 minutes
73
How is remifentanyl metabolized?
plasma and tissue esterases
74
How can remifentanyl be used?
RBB, continuous drip; quick recovery cases
75
What is the dose and drip rate for remifantanyl for DL?
0.5-1mcg/kg, then 0.25-0.5 mcg/kg/min
76
What are the uses of codeine?
antitussiveanalgesia for mild to moderate pain
77
What are the uses for methadone?
long term relief of chronic pain and opioid withdrawl
78
How does dilaudid compare to morphine?
8x as potent but shorter acting
79
What type of drugs are Pantozocine, butorphanol and nalbuphine? What are the advantage?
Partial agonist and/or competitive antagonist at opioid receptorsProduce analgesia with limited respiratory depression, but do have a ceiling effect
80
Name two opioid antagonists and routes of administration.
Nalaxone-IVNaltrexone-po
81
Which opioid receptors does nalaxone antagonize?
pure Mu antagonist
82
What is the duration of nalaxone?
30-45 minutes
83
What is the dose of nalaxone?
1-4mcg/kgDilute 400mcg vial in 100 and give 1-2 cc over 2-3 minutes
84
What are the side effects of nalaxone?
N/VPaintachycardiaIncreased SNS activity

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