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Anesthesia Pharm - Spring 2025 > 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

How potent is Pentazocine?

A
  • 1/5 as potent as morphine
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4
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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5
Q

How is pentazocine excreted?

A
  • Glucuronide conjugates in the urine.
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6
Q

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

A

Pentazocine

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7
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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8
Q

Where is butorphanol excreted?

A

Bile

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9
Q

What receptors does butorphanol bind to?

A
  • κ = analgesia & anti-shivering
  • μ (low)
  • σ (low)
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10
Q

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

A

Dysphoria

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11
Q

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

A

10

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12
Q

By what route is butorphanol rapidly and completely absorbed?

A

Intramuscular

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13
Q

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

A
  • Nalbuphine
  • No increase in BP, pBP, HR.
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14
Q

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

A
  • μ receptor agonist that is equipotent to morphine.
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15
Q

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

A

Buprenorphine

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16
Q

What is buprenorphine’s onset?
Duration?

A
  • 30min onset
  • 8 hour duration
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17
Q

What is buprenorphine’s greatest use?

A
  • Opioid use disorder (has low risk of abuse)
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18
Q

Which two drugs have resistance to naloxone?

A
  • Buprenorphine and Bremazocine.
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19
Q

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

A

Nalorphine

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20
Q

Which drugs are pure μ-opioid receptor antagonists?

A
  • Naloxone
  • Naltrexone
  • Nalmefene
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21
Q

What receptors is naloxone effective on?

A
  • μ, κ, δ (non-selective)
22
Q

What non-opioid uses does naloxone have?

A
  • ↑ contractility for shock
  • Antagonism of general anesthesia at high doses.
23
Q

What is the naloxone IV push dose?
Continuous infusion?

A
  • 1-4 mcg/kg IV
  • 5 mcg/kg IV infusion
24
Q

What dose of naloxone is use for shock?

A
  • > 1mg/kg IV
25
How long does Naloxone last?
- 30 - 45 minutes *Often needs redosing for overdoses*.
26
What are the possible side-effects of naloxone?
- **Analgesia reversal** - **N/V** - ↑ SNS ( ↑ HR, BP, dysrhythmias, etc.)
27
What use does naltrexone have? How long does it last and how is it adminstered?
- EtOH - Given PO (more effective) lasts for 24 hours.
28
How does nalmefene's potency compare to naloxone? What is it's dose and max?
- Nalmefene = naloxone - 15 - 25 mcg IV (max of 1 mcg/kg)
29
What is methylnaltrexone's use?
- Anti-emetic (antagonizes N/V from opioids)
30
What is Alvimopan and what is it used for? How is it metabolized? Why can't it be used long term?
- μ-selective PO peripheral opioid antagonist for **post-op ileus**. - Gut flora metabolism - CV problems long term
31
What are the abuse-resistant opioid formulations?
- Suboxone (buprenorphine + naloxone) - Embeda (long-release morphine + naltrexone) - OxyNal (oxycodone + naltrexone)
32
What opioids-agonists have a significant effect on volatile anesthetics? What do they do?
- Fentanyl & it's derivatives decrease the MAC of volatiles by 50% or greater.
33
Fentanyl 3 μg/kg IV 25-30 min prior to incision will have what effect on which volatile gasses?
- 50% MAC reduction for isoflurane and desflurane.
34
Which opioid partial agonists have an effect on MAC?
- Pentazocine - Butorphanol - Nalbuphine
35
Where are receptors targeted with opioid neuraxial anesthesia?
- Opioid receptors of the substantia gelatinosa.
36
What is general rule of dosing for epidural opioids?
- Dose = 5 - 10 x normal
37
Diffusion of opioids across the _____ ______ results in systemic absorption.
dura mater
38
Where can opioids be injected during an epidural that results in systemic absorption? What should be done if this occurs?
- Epidural venous plexus - Add epi to the infusion.
39
What is Cephalad movement (in regards to epidurals)?
Cephalad Movement = the movement of drug/injectate up the spinal cord towards the brain.
40
What drug attribute decreases cephalad movement?
- Lipid solubility
41
________ exhibits much more cephalad movement than __________. Why is this?
- Morphine ; fentanyl - Fentanyl and it's derivatives are much more lipid soluble and thus exhibit less cephalad movement.
42
What can cause cephalad movement? (besides characteristics of drugs themselves)
Coughing and/or straining
43
When would epidural CSF levels peak for the following drugs: - Fentanyl - Sufentanil - Morphine
- Fentanyl - 20min - Sufentanil - 6min - Morphine - 1-4 hours
44
When would epidural administered plasma levels peak for the following drugs: - Fentanyl - Sufentanil - Morphine
- Fentanyl - 5-10 min - Sufentanil - 5 min or less - Morphine - 10 - 15 min
45
When would epidural administered intrathecal/cervical CSF levels peak for the following drugs: - Fentanyl - Sufentanil - Morphine
- Fentanyl - N/A - Sufentanil - N/A - Morphine - 1 - 5 hours (due to cephalad movement)
46
What is the most common side effect from neuraxial opioid administration? Why does this occur?
- Pruritis - Cephalad migration to trigeminal nucleus
47
What are the treatments for pruritis induced by neuraxial opioids?
- 10mg **Propofol** - Naloxone - Antihistamines - Gabapentin
48
Name the list (its a lot) of side effects that can occur with neuraxial opioid administration.
- Pruritis - N/V - Urinary retention - Respiratory depression - Sedation - Skeletal muscle rigidity - Herpes virus reactivation - Neonatal effects.
49
If neuraxial opioids induced a reemergence of a herpes virus, how long would this occur after opioid administration?
- 2 - 5 days
50
What sign would indicate respiratory depression from neuraxial opioid administration? What is the treatment?
- ↓LOC from ↑CO₂ - Naloxone 0.25 μg/kg/hr IV

Anesthesia Pharm - Spring 2025 (20 decks)

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