Opioids and Opioid Antangonists Flashcards Preview

Anesthesia Pharmacology > Opioids and Opioid Antangonists > Flashcards

Flashcards in Opioids and Opioid Antangonists Deck (83)
1

What is a natural opioid and give example

Naturally derived from opium
morphine

2

What is a synthetic opioid and give example

Manufactured by synthesis
fentanyl

3

What is a semisynthetic opioid and give example

Chemical modification of morphine
herioin

4

What type of receptors do opioids bind?

G coupled protein receptors

5

Where in the body do opioids bind to receptors?

brain and spinal cord

6

What are the endogenous opioid ligands?

Enkephalins
Endorpins
Dynorphins

7

How do opioids affect neurotransmitter release?

decrease

8

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

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

9

where is the mu1 receptor located?

supraspinal and spinal

10

What are the effects of the Mu1 receeptor?

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

11

What binds to the Mu1 receptor?

Endorphins, morphine and sythetic opioids

12

Where is the Mu2 receptor?

spinal

13

What are the effects of the Mu2 receptor?

Hypoventilation
analgesia
Euphoria, Sedation
Physical dependence
Constipation

14

What binds to MU2 receptor?

Endorphins, morphine and sythetic opioids?

15

Where is the kappa receptor?

Supraspinal, spinal

16

What are the effects of the kappa receptor?

Analgesia
Respiratory depression
Dysphoria
diuresis

17

What binds to the kappa receptor?

Dynorphins
Agonist-antagonist principally
Nalbuphine

18

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

resistant

19

Where are the delta opioid receptors?

supraspinal, spinal

20

What are the effects of the delta receptor?

Analgesia
Respiratory depression
Physical dependence
Urinary retention

21

What binds to delta receptors?

enkaphalins

22

Which receptors cause respiratory depression?

Mu2, Kappa, and delta

23

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

Kappa

24

which receptor is associated with constipation?

Mu2

25

Which receptors are associated with physical dependence?

Mu2 and Delta
(kappa has low abuse potential)

25

what are the 4 classic side effects of neuraxial opioids?

Pruritis
N/V
Urinary retention
Ventilatory depression

26

Are neuraxial opioid specific or somatic or visceral pain?

visceral

27

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 contractility
Merperidine is the exception, it has anti muscarinic effects

28

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

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

29

What effect do opioids have on cough?

supress

30

What effects do opioids have on MAC?

reduce

31

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

Decrease CBF and CMRO2
ICP increases due to increase PaCO2 from hypoventilation

32

Which opioid may cause siezures?

Merperidine, from accumulation of normerperidine

33

What is biliary colic?

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

34

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

nalaxone

35

How do you reverse biliary colic?

Glucagon 2mg IV

36

What are the GI side effects of Opioids?

N/V
constipation
delayed gastric emptying
biliary colic

37

Whar are the GU side effects of opioids?

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

38

Which two opioids cause the most histamine release?

morphine and merperidine

39

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

Miosis--oculomotor nerve

40

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

truncal rigidity

41

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

Constipation and miosis

42

What are the triad of symptoms for an opioid overdose?

Miosis
Respiratory depression
Coma

43

What is the onset of morphine?

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

44

What is the peak effect of morphine?

45-90 min

45

What is the duration of morphine?

3-4 hours

46

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

47

What is the dose for intraoperative analgesia of morphine?

.1/-1mg/kg

48

How does merperidine compare to morphine?

0.1 potency

49

How can merperidine be delivered?

IV, IM or PO?

50

How can morphine be delivered?

IV, IM

51

Wha tis the peak effect and duration time for merperidine?

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

52

How does merperidine behave like atropine/local?

blocks sodium channel
causes tachycardia, dry mouth, mydriasis

53

How is merperidine metabolized?

90% hepatic metabolism to normeperidine, which is renally eliminated

54

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

12.5-25mg--1 time dose

55

how does fentanyl compare to morphine?

75-125 times more potent

56

Waht is the peak ffect and duration of fentanyl?

peak: 3-5 minutes
duration 30-60 min

57

how can fentanyl be administered?

IV, transdermal, PO, intranasal

58

Fentanyl is _____ soluble and protein bound

lipid

59

Where is the first pass uptake of fentanyl?

lungs--up to 75%

60

HOw does sufentanil compare to fentanyl?

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

61

what is the peak and duration of sufentanil?

Peak 3-5 minutes, duration 30-60 minutes

62

What is the dose for DL of sufentanil?

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

63

What is the infusion rate for sufentanil?

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

64

How does alfentanyl compare to fentanyl?

1/10-1/5 as potent

65

What is the duration and peak of alfentanyl?

Peak 1.5-2 minutes
Duration 10-20

66

HOw does renal failure affect Alfentanyl?

does not alter clearance

67

What are the uses for alfentanyl?

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

68

What is the dose for alfentanyl?

5-10 mcg/kg

69

How does remifentanyl compare to fentanyl?

similar potency

70

What is the peak effect and duration of remifentanyl?

peak 1.5-2 minutes
Duration 6-12 minutes

71

How is remifentanyl metabolized?

plasma and tissue esterases

72

How can remifentanyl be used?

RBB, continuous drip; quick recovery cases

73

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

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

74

What are the uses of codeine?

antitussive
analgesia for mild to moderate pain

75

What are the uses for methadone?

long term relief of chronic pain and opioid withdrawl

76

How does dilaudid compare to morphine?

8x as potent but shorter acting

77

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

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

78

Name two opioid antagonists and routes of administration.

Nalaxone-IV
Naltrexone-po

79

Which opioid receptors does nalaxone antagonize?

pure Mu antagonist

80

What is the duration of nalaxone?

30-45 minutes

81

What is the dose of nalaxone?

1-4mcg/kg
Dilute 400mcg vial in 100 and give 1-2 cc over 2-3 minutes

82

What are the side effects of nalaxone?

N/V
Pain
tachycardia
Increased SNS activity