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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
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

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