Opioids Flashcards

1
Q

What is a classical analgesic receptor?

A

mu receptor

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2
Q

What are opioids a mix of?

A

Agonist-antagonist agents

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3
Q

What is an opiate? What are some examples?

A

Natural agents from opium

Codeine, morphine

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4
Q

What are opioids?

A

Modifications of natural opiates (synthetics)

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5
Q

What are some examples of mixed opioid agonists?

A

Buprenorphine
Butorphanol
Pentazocine
Nalbuphine

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6
Q

Are mixed agents frequently or infrequently used?

A

Little used

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7
Q

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

A

Nalbuphine

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8
Q

Describe nalbuphine

A

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

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9
Q

What are endorphins derived from?

A

Small endogenous peptide hormones

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10
Q

What do endorphins account for?

A

Variability of response to pain

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11
Q

List the SEs to opiates/opioids

A
Nausea
Itching
Sedation & cognitive impairments
Respiratory depression (possibly life-threatening)
Meiosis (pinpoint pupils)
Decreased GI peristalsis -> constipation
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12
Q

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

A

Anticipate and prophylax

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13
Q

Can we expect tolerance to opioid constipation?

A

No

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14
Q

Review slide 42

A

Bowel regimens for opioid constipation

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15
Q

What opioids do we use for mild-moderate pain?

A

Tramadol
Codeine
Hydrocodone

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16
Q

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

A

Weak opioid analgesic

Useful for chronic pain

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17
Q

What are the 3 forms of tramadol?

A

Immediate release
Tramadol 37.5mg/acetaminophen 325 mg
ER tabs

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18
Q

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

A

High incidence of NV

Limits use for acute pain

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19
Q

Does tramadol have a single or dual MOA

A

Dual

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20
Q

What is tramadol useful for?

A

Neuropathic pain

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21
Q

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

A

Yes
Less abuse potential
2014

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22
Q

What kind of opiate is codeine?

A

Weak analgesic and antitussive

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23
Q

Relate codeine to ASA

A

60 mg less effective than 650 mg aspirin

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24
Q

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

A

CYP2D6

Morphine

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25
Q

What does CYP2D6 inhibitors do to codeine? Give some examples

A
Decrease its effect
Antiemetic phenothiazines (thorazine, compazine, phenergan)
Haloperidol
Fluoxetine
Paroxetine
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26
Q

What % of the population lack the CYP2D6 enzyme?

A

10%

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27
Q

What forms does codeine come in?

A

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

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28
Q

How is hydrocodone available PO?

A

Only available w/ acetaminophen PO

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29
Q

How many mg does hydocodone exist w/in Norco?

A

325 mg

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30
Q

Give two more examples of hydrocodone PO meds

A

Lortab

Vicoden

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31
Q

How does hydrocodone relate to codeine?

A

Better pain relief

Longer duration

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32
Q

What is hydrocodone metabolized by and to what?

A

CYP2D6

Hydromorphone

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33
Q

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

A

63%

Hydrocodone

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34
Q

What opioids do we give for moderate to severe pain?

A
Morphine
Hydromorphone
Oxycodone
Meperidine
Methadone
Fentanyl
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35
Q

What type of drug is morphine?

A

Prototype pure mu receptor agonist

36
Q

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

A

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

37
Q

What does morphine induce? What happens because of that?

A

Histamine release

Hypotension, pruritus

38
Q

What kind of first-pass effect does morphine have?

A

Significant

39
Q

What is the parenteral to oral dose ratio of morphine?

A

1:3

40
Q

What is the concentration of injectable morphine?

A

2 mg/mL

41
Q

Give the examples of oral morphine

A
Immediate release tabs
SR capsules (Kadian)
CR tabs (MS Contin)
Oral solution (roxanol)
42
Q

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

A

5-7

Often forgotten by prescribers -> results in iatrogenic overdoses

43
Q

What are two benefits of hydromorphone?

A

Less histamine release

No active opioid metabolites

44
Q

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

A

8
12
16
32 mg

45
Q

Why was SR palladone recalled by the FDA?

A

Alcohol destroyed time-release mechanism, which led to overdoses

46
Q

What is a common concentration of hydromorphone injections?

A

2 mg/mL

47
Q

How does oxycodone relate to morphine?

A
More potent
Less SEs (histamine release, pruritus, N)
48
Q

What is oxycodone metabolized to and by what?

A

Oxymorphone

CYP2D6

49
Q

What pt populations is oxycodone helpful with?

A

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

50
Q

Give some examples of oxycodone dosage forms

A

Oxycodone IR
Roxicodone
Oxycodone CR

51
Q

How do you administer oxycodone CR and how often?

A

Q12 hours PO

52
Q

Is meperidine a 1st line agent?

A

No

53
Q

Describe the qualities of meperidine

A

Lipophilic
Rapid onset
Shorter duration (2-3 hours)

54
Q

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

A

Normeperidine

Its neurotoxic

55
Q

Does normeperidine have a long or short half life?

A

Long

56
Q

What are the indications of noremperidine toxicity?

A

Euphoria
Irritability
Seizures

57
Q

Is normeperidine toxicity reversible by opiate antagonists?

A

No

58
Q

How is normeperidine eliminated?

A

Renally

59
Q

When is meperidine contraindicated? What does it cause?

A

Pts on MAOIs

Serotonin syndrome

60
Q

When can meperidine be used?

A

In pts w/ opiate allergies

61
Q

What is meperidine useful in controlling?

A

Post anesthesia shivering

62
Q

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

A

Racemic mix of L and D isomers

Neuropathic pain

63
Q

What does the L isomer do for methadone?

A

Opioid activity

64
Q

What does the D isomer do for methadone?

A

NMDA antagoinst and NE/5HT reuptake inhbitor

65
Q

Describe the half-life of methadone

A

Very long and variable
12-190 hours
Usually about 24

66
Q

How long do methadone’s analgesic effects last?

A

4-8 hours

67
Q

How often do you dose methadone for analgesia?

A

Q6-8 hours

68
Q

How much more potent than morphine is fentanyl?

In what units is it dosed because of this?

A

100 times

Mcg

69
Q

Describe the qualities of fentanyl

A

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

70
Q

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

A

No

One of the safest options in renal failure

71
Q

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

A

Fewer

Minimal histamine release, little hypotensive effect

72
Q

How do we give fentanyl?

A

Injection
Lozenge
Transdermal (duragesic)

73
Q

Review slide 55

A

Duragesic calculator

74
Q

With what pt population do we not use duragesic cautions?

A

Opiate niave pts

75
Q

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

A

First 24 hours

76
Q

When do we replace the duragesic patches?

A

Q 72 hours

77
Q

Do you just add additional patches of duragesic?

A

No

78
Q

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

A

Multiple patches

79
Q

What are the fentanyl lozenges used for?

A

Long-standing chronic pain

cancer

80
Q

What are two fentanyl lozenge products?

A

Fentora

Actiq

81
Q

What kind of drug is naloxone?

A

Pure mu receptor antagonist

82
Q

What is naloxone used for?

A

To reverse sedation/respiratory depression

83
Q

How do you administer naloxone?

A

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
Q

Review slide 60 and 62

A

Equianalgesic dosing and chart

85
Q

Review slide 65

A

Common PCA settings

86
Q

What is oxycodone w/ acetaminophen?

A

Percocet

87
Q

What is oxycodone w/ aspirin?

A

Percodan