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(Steele) Anesthesia Pharm Grayson (Spring 2023) > Opioid Agonist-Antagonists & Antagonists (Exam II) > Flashcards

Opioid Agonist-Antagonists & Antagonists (Exam II) Flashcards

1
Q

What is the primary indication for opioid agonist-antagonists?

A
  • Used if unable to tolerate full agonist
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2
Q

Name the four advantages of opioid agonist-antagonists.

A
  • Analgesia
  • Less respiratory depression
  • Low dependence potential
  • Ceiling effect (prevents ODing)
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3
Q

Opioid antagonists bind to their receptors how?

A

Mu: partial effect (agonist) or No effect (comp. antagonist)
K and delta: partial effect (agonist)

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4
Q

How potent is Pentazocine?

A
  • 1/5 as potent as morphine and Nalorphine
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5
Q

What is the gold standard for opioid agonist-antagonists?

A

Nalorphine

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6
Q

What receptors does pentazocine bind to?
What type of activity does it exhibit?

A
  • κ & δ receptor partial agonist activity
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7
Q

How is pentazocine excreted?

A
  • Glucuronide conjugates in the urine.
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8
Q

Which opioid agonist-antagonist crosses the placental barrier causing fetal depression?

A

Pentazocine

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9
Q

What is the chronic pain dose of Pentazocine?
What dose and route would be equivalent to morphine 10mg?

A
  • 10 - 30mg IV or 50 mg PO
  • 20-30mg IM = 10mg morphine
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10
Q

Where is butorphanol excreted?

A

Bile > urine

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11
Q

What receptors does butorphanol bind to?

A
  • κ = analgesia & anti-shivering
  • μ (low)
  • Sigma = σ (low)
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12
Q

Sigma (σ) receptors are associated with what side effect?

A

Dysphoria

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13
Q

2 to 3 mg of butorphanol is equivalent to _____ mg of morphine.

A

10

(depression of ventilation)

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14
Q

Which receptor has a moderate affinity for Butorphanol’s effects to mitigate shivering and produce analgesia?

A. Mu
B. Kappa
C. Sigma
D. Delta

A

B. Kappa

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15
Q

Pentazocine Side effects: (5)

A
  • sedation
  • diaphoresis
  • dizziness
  • dysphoria (high doses)
  • increased HR, BP, PArtPress, LVEDP with high doses
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16
Q

By what route is butorphanol rapidly and completely absorbed?

A

Intramuscular

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17
Q

Elimination half-time of ____ is 2-3 hrs and it is 2.5-3.5 hrs in _____

A

Pentazocine

Butorphanol

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18
Q

What drug is an excellent choice for cardiac catheterization patients?
Why?

A
  • Nalbuphine
  • No increase in BP, pBP, HR or Atrial filling pressures
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19
Q

What receptors does nalbuphine bind to?
How potent is it?

A
  • μ receptor agonist that is equipotent to morphine.
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20
Q

Which agonist-antagonist has 50 times greater μ receptor affinity than morphine?

A

Buprenorphine

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21
Q

What is buprenorphine’s onset?
Duration?

A
  • 30min onset
  • 8 hour duration
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22
Q

0.3 Mg IM of Buprenorphine =

A

10 mg of morphine

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23
Q

What is buprenorphine’s greatest use?

A
  • Opioid use disorder (has low risk of abuse)
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24
Q

What are 3 side effects of Buprenorphine?

A
  • Pulmonary edema
  • withdrawal
  • low risk of abuse
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25
Q

Which two drugs have resistance to naloxone?

A
  • Buprenorphine and Bremazocine.
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26
Q

Which opioid has high incidence of dysphoria and is therefore not utilized clinically?

A

Nalorphine

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27
Q

which drug is 25% bound to protein, …

A

Meptazinol

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28
Q

which drug has 2x potency than morphine at the K receptors?

A

Bremazocine

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29
Q

Which drugs are pure μ-opioid receptor antagonists?

A
  • Naloxone
  • Naltrexone
  • Nalmefene
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30
Q

Which Opioid Agonist-Antagonist is more potent than Morphine?

A. Nalorphine
B. Nalbuphine
C. Buprenorphine
D. Meptazinol

A

Buprenorphine

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31
Q

What receptors is naloxone effective on?

A
  • μ, κ, δ (non-selective)
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32
Q

Which drugs are competitive antatgonists for µ opioid receptors and has high affinity for it?

A

Naloxone, Naltrexone, and Nalmefene

33
Q

What non-opioid uses does naloxone have?

A
  • ↑ contractility for shock
  • Antagonism of general anesthesia at high doses.
34
Q

What is the dose for Naloxone?

A

1 to 4 µg/kg IV
5 µg/kg IV continuous infusion

35
Q

What dose of naloxone is use for shock?

A
  • > 1mg/kg IV
36
Q

How long does Naloxone last?

A
  • 30 - 45 minutes

Often needs redosing for overdoses.

37
Q

Metabolism of this drug is by the liver, has an elimination half-time of 60-90 min and the hepatic first pass is 1/5th PO

38
Q

What are the possible side-effects of naloxone? (5)

A
  • Analgesia reversal
  • N/V
  • ↑ SNS ( ↑ HR, BP)
  • Pulmonary edema
  • dysrhythmias (v-fib)
39
Q

What use does naltrexone have?
How long does it last and how is it adminstered?

A
  • EtOH
  • Given PO (more effective) lasts for 24 hours.
40
Q

How does nalmefene’s potency compare to naloxone?
What is it’s dose and max?

A
  • Nalmefene = naloxone
  • 15 - 25 mcg IV (max of 1 mcg/kg)
41
Q

Half-time of this drug is 10.8 hrs

42
Q

What is methylnaltrexone’s use?

A
  • Anti-emetic (antagonizes N/V from opioids)
  • promotes gastric emptying
43
Q

What is Alvimopan and what is it used for?
How is it metabolized?
Why can’t it be used long term?

A
  • μ-selective PO peripheral opioid antagonist for post-op ileus.
  • Gut flora metabolism
  • CV problems with long term use
44
Q

What are the abuse-resistant opioid formulations?

A
  • Suboxone (buprenorphine + naloxone)
  • Embeda (long-release morphine + naltrexone)
  • OxyNal (oxycodone + naltrexone)
45
Q

What opioid-agonists have a significant effect on volatile anesthetics?

A
  • Fentanyl & it’s derivatives decrease the MAC of volatiles by 50% or greater.
46
Q

Fentanyl 3 μg/kg IV 25-30 min prior to incision will have what effect on which volatile gasses?

A
  • 50% MAC reduction for isoflurane and desflurane.
47
Q

Sufentanil decreases MAC with Enflurane by

48
Q

Alfentanil decreases MAC by

49
Q

Remifentanil decreases MAC by

50
Q

Which opioid partial agonists have an effect on decreasing MAC?

A
  • Pentazocine
  • Butorphanol
  • Nalbuphine
51
Q

Where are receptors targeted with opioid neuraxial anesthesia?

A
  • Opioid receptors of the substantia gelatinosa.
52
Q

What is general rule of dosing for epidural opioids?

A
  • Dose = 5 - 10 x normal
53
Q

Name the three blanks

54
Q

Diffusion of opioids across the _____ ______ results in systemic absorption.

A

dura mater

55
Q

Neuraxial opioids do not cause

A

Sympathectomy
sensory block
weakness

56
Q

Where can opioids be injected during an epidural that results in systemic absorption?
What should be done if this occurs?

A
  • Epidural venous plexus
  • Add epi or neo to the infusion.
57
Q

Spinal/Intrathecal/Subarachnoid Block (SAB) are ___

A

all interchangeable

58
Q

Epidural uptake takes place in

slide 34

A

Uptake in the fat
in the venous plexus = systemic aborption

59
Q

The goal of the epidural is to ____

A

have it cross the dura and enter the or bath the CSF

60
Q

Fent epidural
Peak:
Strenght compared to morphine

A

Peak: 20 min

Fent is 800x stronger than morphine

61
Q

Sufentanil epidural
Peak:
Strenght compared to morphine

A

Peak: 6 min

Sufentanil is 1600x stronger than morphine

62
Q

What is Cephalad movement (in regards to epidurals)?

A

Cephalad Movement = the movement of drug/injectate up the spinal cord towards the brain.

63
Q

What drug attribute decreases cephalad movement?

A
  • the higher the Lipid solubility –> the less cephalad movement (up)
64
Q

T1 - T4 are our ____ _____

A

Cardiac accelorators

64
Q

PCA doses for Fentanyl
Basal rate:
Bolus dose:
Bolus interval (min):

A

Basal rate: 0 - 60 mcg/hr
Bolus dose: 20 - 50 mcg
Bolus interval (min): 5 - 10 min

65
Q

What is shown here?

A

The lack of oversedation and dip into longer pain with PCA administration compared to PRN administration

66
Q

PCA doses for morphine
Basal rate:
Bolus dose:
Bolus interval (min):

A

Basal rate: 0-2 mg/hr
Bolus dose: 1-2 mg
Bolus interval (min): 6-10 min

67
Q

PCA doses for Hydromorphone
Basal rate:
Bolus dose:
Bolus interval (min):

A

Basal rate: 0-0.4 mg/hr
Bolus dose: 0.2-0.4 mg
Bolus interval (min): 6-10 min

68
Q

________ exhibits much more cephalad movement than __________.
Why is this?

A
  • Morphine ; fentanyl
  • Fentanyl and it’s derivatives are much more lipid soluble and thus exhibit less cephalad movement.
69
Q

What can cause cephalad movement? (besides characteristics of drugs themselves)

A

Coughing and/or straining

70
Q

When would epidural CSF levels peak for the following drugs:
- Fentanyl
- Sufentanil
- Morphine

A
  • Fentanyl - 20min
  • Sufentanil - 6min
  • Morphine - 1-4 hours
71
Q

When would epidural administered plasma levels peak for the following drugs:
- Fentanyl
- Sufentanil
- Morphine

A
  • Fentanyl - 5-10 min
  • Sufentanil - 5 min or less
  • Morphine - 10 - 15 min
72
Q

For Neuraxial morphine
CSF peak time:
Plasma peak time:
cervical/CSF levels maintained for:

A

CSF peak time: 1-4 hrs
Plasma peak time: 10-15 min
cervical/CSF levels maintained for: 1-5 hrs

73
Q

When would epidural administered intrathecal/cervical CSF levels peak for the following drugs:
- Fentanyl
- Sufentanil
- Morphine

A
  • Fentanyl - N/A
  • Sufentanil - N/A
  • Morphine - 1 - 5 hours (due to cephalad movement)
74
Q

What is the most common side effect from neuraxial opioid administration?
Why does this occur?

A
  • Pruritis
  • Cephalad migration to trigeminal nucleus
75
Q

What are the treatments for pruritis induced by neuraxial opioids? (4)

A
  • 10mg Propofol
  • Naloxone
  • Antihistamines
  • Gabapentin
76
Q

Name the list (its a lot) of side effects that can occur with neuraxial opioid administration. (8)

A
  • Pruritis
  • N/V
  • Urinary retention (males)
  • Respiratory depression
  • Sedation
  • Skeletal muscle rigidity
  • Herpes virus reactivation
  • Neonatal effects.
77
Q

If neuraxial opioids induced a reemergence of a herpes virus, how long would this occur after opioid administration?

A
  • 2 - 5 days
78
Q

What sign would indicate respiratory depression from neuraxial opioid administration?

What is the treatment?

A
  • ↓LOC from ↑CO₂
  • Naloxone 0.25 μg/kg/hr IV

(Steele) Anesthesia Pharm Grayson (Spring 2023) (20 decks)

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