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Anesthesia Pharmacology > Opioids and Opioid Antangonists > Flashcards

Opioids and Opioid Antangonists Flashcards

1
Q

What is a natural opioid and give example

A

Naturally derived from opium

morphine

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2
Q

What is a synthetic opioid and give example

A

Manufactured by synthesis

fentanyl

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3
Q

What is a semisynthetic opioid and give example

A

Chemical modification of morphine

herioin

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4
Q

What type of receptors do opioids bind?

A

G coupled protein receptors

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5
Q

Where in the body do opioids bind to receptors?

A

brain and spinal cord

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6
Q

What are the endogenous opioid ligands?

A

Enkephalins
Endorpins
Dynorphins

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7
Q

How do opioids affect neurotransmitter release?

A

decrease

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8
Q

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

A 
Periaqueductal gray matter
amygdala
Corpus striatum
Hypothalamus
Spinal cord (substantia gelatinosa)
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9
Q

where is the mu1 receptor located?

A

supraspinal and spinal

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10
Q

What are the effects of the Mu1 receeptor?

A 
Analgesia--main action
Euphoria
N/V, Pruritis
Low abuse potential
Bradycardia
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11
Q

What binds to the Mu1 receptor?

A

Endorphins, morphine and sythetic opioids

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12
Q

Where is the Mu2 receptor?

A

spinal

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13
Q

What are the effects of the Mu2 receptor?

A 
Hypoventilation
analgesia
Euphoria, Sedation
Physical dependence
Constipation
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14
Q

What binds to MU2 receptor?

A

Endorphins, morphine and sythetic opioids?

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15
Q

Where is the kappa receptor?

A

Supraspinal, spinal

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16
Q

What are the effects of the kappa receptor?

A

Analgesia
Respiratory depression
Dysphoria
diuresis

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17
Q

What binds to the kappa receptor?

A

Dynorphins
Agonist-antagonist principally
Nalbuphine

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18
Q

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

A

resistant

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19
Q

Where are the delta opioid receptors?

A

supraspinal, spinal

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20
Q

What are the effects of the delta receptor?

A

Analgesia
Respiratory depression
Physical dependence
Urinary retention

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21
Q

What binds to delta receptors?

A

enkaphalins

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22
Q

Which receptors cause respiratory depression?

A

Mu2, Kappa, and delta

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23
Q

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

A

Kappa

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24
Q

which receptor is associated with constipation?

A

Mu2

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25
Q

Which receptors are associated with physical dependence?

A

Mu2 and Delta

kappa has low abuse potential

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25
Q

what are the 4 classic side effects of neuraxial opioids?

A

Pruritis
N/V
Urinary retention
Ventilatory depression

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26
Q

Are neuraxial opioid specific or somatic or visceral pain?

A

visceral

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27
Q

What are the cardiovascular effects of most opioids?

What is the exception?

A

decrease sympathetic tone and therefore decrease BP, HR. There are minimal effects on the contractility
Merperidine is the exception, it has anti muscarinic effects

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28
Q

How do opioids affect RR, Vt, MV, and PaCO2?

A

Decrease RR, INcrease Vt, but overall decreases MV, and thus increases PaCO2

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29
Q

What effect do opioids have on cough?

A

supress

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30
Q

What effects do opioids have on MAC?

A

reduce

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31
Q

What effects do opioids have on cerebral blood flow, metabolic rate and ICP?

A

Decrease CBF and CMRO2

ICP increases due to increase PaCO2 from hypoventilation

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32
Q

Which opioid may cause siezures?

A

Merperidine, from accumulation of normerperidine

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33
Q

What is biliary colic?

A

Spasm of the sphincter of Oddi
Feels similar to angina
If not relieved by NTG then it is biliary colic

34
Q

What can you give to relieve pain associated with biliary colic?

A

nalaxone

35
Q

How do you reverse biliary colic?

A

Glucagon 2mg IV

36
Q

What are the GI side effects of Opioids?

A

N/V
constipation
delayed gastric emptying
biliary colic

37
Q

Whar are the GU side effects of opioids?

A

Urinary retention due to increase in tone of ureter and vesicle sphincter

38
Q

Which two opioids cause the most histamine release?

A

morphine and merperidine

39
Q

what opioid side effect is associated with the Erdinger-Westphal nucleus?

A

Miosis–oculomotor nerve

40
Q

What side effect of opioids is associated with difficulty to bag mask pt?

A

truncal rigidity

41
Q

Which two effects of opioids aren’t subject to tolerance?

A

Constipation and miosis

42
Q

What are the triad of symptoms for an opioid overdose?

A

Miosis
Respiratory depression
Coma

43
Q

What is the onset of morphine?

A

15-30 min onset with peak effect at 45-90 min

44
Q

What is the peak effect of morphine?

A

45-90 min

45
Q

What is the duration of morphine?

A

3-4 hours

46
Q

How is morphine metabolized? What is the metabolite and how does it compare to morphine?

A

Metabolized via conjugation with glucuronic acid in liver and in kidney.
Its metabolite is morphine-6-gucuronide, which is more potent than morphine

47
Q

What is the dose for intraoperative analgesia of morphine?

A

.1/-1mg/kg

48
Q

How does merperidine compare to morphine?

A

0.1 potency

49
Q

How can merperidine be delivered?

A

IV, IM or PO?

50
Q

How can morphine be delivered?

A

IV, IM

51
Q

Wha tis the peak effect and duration time for merperidine?

A

Peak: 5-7 min
Duration: 2-4 hours

52
Q

How does merperidine behave like atropine/local?

A

blocks sodium channel

causes tachycardia, dry mouth, mydriasis

53
Q

How is merperidine metabolized?

A

90% hepatic metabolism to normeperidine, which is renally eliminated

54
Q

What is the dose of merperidine for post-op shivering?

A

12.5-25mg–1 time dose

55
Q

how does fentanyl compare to morphine?

A

75-125 times more potent

56
Q

Waht is the peak ffect and duration of fentanyl?

A

peak: 3-5 minutes

duration 30-60 min

57
Q

how can fentanyl be administered?

A

IV, transdermal, PO, intranasal

58
Q

Fentanyl is _____ soluble and protein bound

A

lipid

59
Q

Where is the first pass uptake of fentanyl?

A

lungs–up to 75%

60
Q

HOw does sufentanil compare to fentanyl?

A

5-10x as potent with greater affinity for opioid receptor

61
Q

what is the peak and duration of sufentanil?

A

Peak 3-5 minutes, duration 30-60 minutes

62
Q

What is the dose for DL of sufentanil?

A

0.3-1mcg/kg 1-3 minutes before DL

63
Q

What is the infusion rate for sufentanil?

A

0.5 mcg/kg followed by 0.5 mcg/kg/hr

64
Q

How does alfentanyl compare to fentanyl?

A

1/10-1/5 as potent

65
Q

What is the duration and peak of alfentanyl?

A

Peak 1.5-2 minutes

Duration 10-20

66
Q

HOw does renal failure affect Alfentanyl?

A

does not alter clearance

67
Q

What are the uses for alfentanyl?

A

Because of its rapid on and off of intense analgesia, it is good for retrobulbar block or DL

68
Q

What is the dose for alfentanyl?

A

5-10 mcg/kg

69
Q

How does remifentanyl compare to fentanyl?

A

similar potency

70
Q

What is the peak effect and duration of remifentanyl?

A

peak 1.5-2 minutes

Duration 6-12 minutes

71
Q

How is remifentanyl metabolized?

A

plasma and tissue esterases

72
Q

How can remifentanyl be used?

A

RBB, continuous drip; quick recovery cases

73
Q

What is the dose and drip rate for remifantanyl for DL?

A

0.5-1mcg/kg, then 0.25-0.5 mcg/kg/min

74
Q

What are the uses of codeine?

A

antitussive

analgesia for mild to moderate pain

75
Q

What are the uses for methadone?

A

long term relief of chronic pain and opioid withdrawl

76
Q

How does dilaudid compare to morphine?

A

8x as potent but shorter acting

77
Q

What type of drugs are Pantozocine, butorphanol and nalbuphine? What are the advantage?

A

Partial agonist and/or competitive antagonist at opioid receptors
Produce analgesia with limited respiratory depression, but do have a ceiling effect

78
Q

Name two opioid antagonists and routes of administration.

A

Nalaxone-IV

Naltrexone-po

79
Q

Which opioid receptors does nalaxone antagonize?

A

pure Mu antagonist

80
Q

What is the duration of nalaxone?

A

30-45 minutes

81
Q

What is the dose of nalaxone?

A

1-4mcg/kg

Dilute 400mcg vial in 100 and give 1-2 cc over 2-3 minutes

82
Q

What are the side effects of nalaxone?

A

N/V
Pain
tachycardia
Increased SNS activity

Anesthesia Pharmacology (25 decks)

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