Opioids Flashcards Preview

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Flashcards in Opioids Deck (87):
1

What is a classical analgesic receptor?

mu receptor

2

What are opioids a mix of?

Agonist-antagonist agents

3

What is an opiate? What are some examples?

Natural agents from opium
Codeine, morphine

4

What are opioids?

Modifications of natural opiates (synthetics)

5

What are some examples of mixed opioid agonists?

Buprenorphine
Butorphanol
Pentazocine
Nalbuphine

6

Are mixed agents frequently or infrequently used?

Little used

7

What is an exception to the little use of mixed opioid agonist-antagoinsts?

Nalbuphine

8

Describe nalbuphine

More effective in females
Ceiling effect on respiratory depression
Used in L&D

9

What are endorphins derived from?

Small endogenous peptide hormones

10

What do endorphins account for?

Variability of response to pain

11

List the SEs to opiates/opioids

Nausea
Itching
Sedation & cognitive impairments
Respiratory depression (possibly life-threatening)
Meiosis (pinpoint pupils)
Decreased GI peristalsis -> constipation

12

How do we deal with the effects of opioids on the GI tract?

Anticipate and prophylax

13

Can we expect tolerance to opioid constipation?

No

14

Review slide 42

Bowel regimens for opioid constipation

15

What opioids do we use for mild-moderate pain?

Tramadol
Codeine
Hydrocodone

16

What kind of opioid is tramadol? What is it useful for?

Weak opioid analgesic
Useful for chronic pain

17

What are the 3 forms of tramadol?

Immediate release
Tramadol 37.5mg/acetaminophen 325 mg
ER tabs

18

What happens as we increase dosage of tramadol over weeks? What does this mean?

High incidence of NV
Limits use for acute pain

19

Does tramadol have a single or dual MOA

Dual

20

What is tramadol useful for?

Neuropathic pain

21

Is tramadol a controlled substance? If so, why? When did this happen if it did?

Yes
Less abuse potential
2014

22

What kind of opiate is codeine?

Weak analgesic and antitussive

23

Relate codeine to ASA

60 mg less effective than 650 mg aspirin

24

What is codeine metabolized by? What does this metabolize codeine to?

CYP2D6
Morphine

25

What does CYP2D6 inhibitors do to codeine? Give some examples

Decrease its effect
Antiemetic phenothiazines (thorazine, compazine, phenergan)
Haloperidol
Fluoxetine
Paroxetine

26

What % of the population lack the CYP2D6 enzyme?

10%

27

What forms does codeine come in?

Codeine (C-II)
Tylenol w/ codeine (C-III)
Guaifenesin w/ codeine (C-V)

28

How is hydrocodone available PO?

Only available w/ acetaminophen PO

29

How many mg does hydocodone exist w/in Norco?

325 mg

30

Give two more examples of hydrocodone PO meds

Lortab
Vicoden

31

How does hydrocodone relate to codeine?

Better pain relief
Longer duration

32

What is hydrocodone metabolized by and to what?

CYP2D6
Hydromorphone

33

What % of unintentional overdoses involve combination products? What is the MC opioid in these combination products?

63%
Hydrocodone

34

What opioids do we give for moderate to severe pain?

Morphine
Hydromorphone
Oxycodone
Meperidine
Methadone
Fentanyl

35

What type of drug is morphine?

Prototype pure mu receptor agonist

36

How many active metabolites does morphine have? How are they eliminated?
What are they?

2
Renally
A neurotoxin and an analgesic 2-4xs that of morphine

37

What does morphine induce? What happens because of that?

Histamine release
Hypotension, pruritus

38

What kind of first-pass effect does morphine have?

Significant

39

What is the parenteral to oral dose ratio of morphine?

1:3

40

What is the concentration of injectable morphine?

2 mg/mL

41

Give the examples of oral morphine

Immediate release tabs
SR capsules (Kadian)
CR tabs (MS Contin)
Oral solution (roxanol)

42

How much more potent is hydromorphone than morphine? What is an issue w/ that?

5-7
Often forgotten by prescribers -> results in iatrogenic overdoses

43

What are two benefits of hydromorphone?

Less histamine release
No active opioid metabolites

44

In what doses do the sustained release products of hydromorphone come in?

8
12
16
32 mg

45

Why was SR palladone recalled by the FDA?

Alcohol destroyed time-release mechanism, which led to overdoses

46

What is a common concentration of hydromorphone injections?

2 mg/mL

47

How does oxycodone relate to morphine?

More potent
Less SEs (histamine release, pruritus, N)

48

What is oxycodone metabolized to and by what?

Oxymorphone
CYP2D6

49

What pt populations is oxycodone helpful with?

PTs w/ CYP2D6 deficiency or on inhibitors (phenothiazine antiemetics, fluoxetine, paroxetine)
Useful in non-responders to codeine and hydrocodone

50

Give some examples of oxycodone dosage forms

Oxycodone IR
Roxicodone
Oxycodone CR

51

How do you administer oxycodone CR and how often?

Q12 hours PO

52

Is meperidine a 1st line agent?

No

53

Describe the qualities of meperidine

Lipophilic
Rapid onset
Shorter duration (2-3 hours)

54

What is meperidine metabolized to? Whys is that a bad thing?

Normeperidine
Its neurotoxic

55

Does normeperidine have a long or short half life?

Long

56

What are the indications of noremperidine toxicity?

Euphoria
Irritability
Seizures

57

Is normeperidine toxicity reversible by opiate antagonists?

No

58

How is normeperidine eliminated?

Renally

59

When is meperidine contraindicated? What does it cause?

Pts on MAOIs
Serotonin syndrome

60

When can meperidine be used?

In pts w/ opiate allergies

61

What is meperidine useful in controlling?

Post anesthesia shivering

62

What makes methadone unique? What is one of its uses?

Racemic mix of L and D isomers
Neuropathic pain

63

What does the L isomer do for methadone?

Opioid activity

64

What does the D isomer do for methadone?

NMDA antagoinst and NE/5HT reuptake inhbitor

65

Describe the half-life of methadone

Very long and variable
12-190 hours
Usually about 24

66

How long do methadone's analgesic effects last?

4-8 hours

67

How often do you dose methadone for analgesia?

Q6-8 hours

68

How much more potent than morphine is fentanyl?
In what units is it dosed because of this?

100 times
Mcg

69

Describe the qualities of fentanyl

Extremely lipophilic
Rapid onset
SHORT duration (30-60 mins)

70

Does fentanyl have any metabolites? What does this mean for use?

No
One of the safest options in renal failure

71

How do the AEs of fentanyl compare to morphine/dilaudid? Describe them

Fewer
Minimal histamine release, little hypotensive effect

72

How do we give fentanyl?

Injection
Lozenge
Transdermal (duragesic)

73

Review slide 55

Duragesic calculator

74

With what pt population do we not use duragesic cautions?

Opiate niave pts

75

How long do we monitor the respiratory rate for pts recieving the duragesic patch?

First 24 hours

76

When do we replace the duragesic patches?

Q 72 hours

77

Do you just add additional patches of duragesic?

No

78

What do you need to look for when admitting out patient pts on the duragesic patch?

Multiple patches

79

What are the fentanyl lozenges used for?

Long-standing chronic pain
*cancer*

80

What are two fentanyl lozenge products?

Fentora
Actiq

81

What kind of drug is naloxone?

Pure mu receptor antagonist

82

What is naloxone used for?

To reverse sedation/respiratory depression

83

How do you administer naloxone?

1) Dilute 0.4 mg to > 10 mL saline (0.9% NaCl)
2) administer via slow IVP (1 mL/1-2 min)
3) Monitor respiratory rate
4) Stop when RR increases

84

Review slide 60 and 62

Equianalgesic dosing and chart

85

Review slide 65

Common PCA settings

86

What is oxycodone w/ acetaminophen?

Percocet

87

What is oxycodone w/ aspirin?

Percodan