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Anes Pharm Spring 2025 > SS25 Opioid Agonist-Antagonists & Antagonists (Exam 2) > Flashcards

SS25 Opioid Agonist-Antagonists & Antagonists (Exam 2) Flashcards

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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 (better for COPD, Obesity, diff. airway)
  • Low dependence potential
  • Ceiling effect
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3
Q

Generalized SE of opioid agonist-antagonists.

A
  • same as morphine + dysphoric reactions (ie: fear of impending death)
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4
Q

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

A

Dysphoria

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5
Q

What is the ceiling effect?

A
  • prevents additional (ie: OD)
  • Drug impacts on body plateaus
  • Higher doses do not increase its effects
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6
Q

Which receptors do opioid agonist-antagonists?

A
  • μ - partial agonist effect or no effect (competitive antagonist)
    κ & σ - partial agonist effect
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7
Q

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

A
  • κ & δ receptor partial agonist activity
  • weak antagonistic effects
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8
Q

How potent is Pentazocine?

A
  • 1/5 (20%) as potent as Nalorphine
  • Nalorphine equally potent to Morphine
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9
Q

Pentazocine: Pharmacokinetics
- First pass?
- E1/2?
- Excretion?

A
  • Hepatic: HIGH (80%)
    - only 20% enters circulation
  • E1/2: 2 - 3 hrs
  • Glucoronide conjugates in the urine
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10
Q

Pentazocine:
- Chronic pain dose IV, IM, & PO?
-Which opioid agonist is the PO dose equal to?
- Which opioid agonist is the IM dose equal?

A
  • IV: 10 - 30mg
  • PO: 50 mg (= Codeine 60 mg PO)
  • IM: 20-30mg (= 10mg of morphine)
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11
Q

T/F: Epidural analgesia administration of Pentazocine has a shorter duration than Morphine.

A
  • True
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12
Q

Pentazocine SE:

A
  • increased HR, BP, PAP, LVEDP
    -sedation
    -diaphoresis
    -dysphoria (at high doses)
  • dizziness
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13
Q

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

A

Pentazocine

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14
Q

What receptors does Butorphanol (Stadol) bind to?
-What responses are elicited?

A
  • κ = (moderate affinity) analgesia & anti-shivering
  • μ (low affinity) - low antagonism
  • σ (low affinity) - low dysphoria
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15
Q

Potency of Butorphanol

A
  • Agonistic: 20x > Pentazocine
    -Antagonistic: 10 - 30 x > Pentazocine
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16
Q

By what route is Butorphanol rapidly and completely absorbed?

A
  • IM
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17
Q

Butorphanol:
PostOp IM dose:
Indications:

A
  • PostOp: 2 - 3 mg IM
  • Use: Typically post op pain, anti-shivering, migraines
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18
Q

2 to 3 mg of butorphanol is equivalent to _____ mg of morphine.
- Why is this clinically significant?

A
  • 10 mg
  • Ventilation depression
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19
Q

Butorphanol:
- Metabolism?
- E1/2?
- Excretion?

A
  • E1/2: 2.5 -3.5 hrs
  • Metabolism: Hepatic
  • Excretion: Bile > urine
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20
Q

Butorphanol SE:

A
  • same typical side effects: sedation, nausea, diaphoresis, dysphoria (less frequent), vent depression, wdl symptoms,** increased HR, BP, PAP,CO**
  • may difficult to use with other opioid agonist
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21
Q

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

A
  • Nalbuphine
  • No increase in BP, PAP, HR, or atrial filling pressures
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22
Q

What receptors does Nalbuphine bind to?
- How potent is it?

A
  • μ receptor agonist
  • Equally potent to morphine (10 mg = 10 mg)
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23
Q

What’s Nalbuphine antagonistic potency?

A
  • 1/4th as potent as Nalorphine
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24
Q

Nalbuphine:
- Metabolism?
- E1/2?
- SE?

A
  • Liver
  • 3 - 6 hrs
  • sedation, dysphoria, wdl symptoms
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25
What receptor(s) does Buprenorphine agonizes? -What is the analgesic potency?
- **μ** receptor agonist - Affinity 50x > Morphine - **0.3 mg IM = 10 mg Morphine**
26
Buprenorphine: - Onset? - Duration?
- Onset: 30 mins - Duration: 8 hrs (**slow dissociation from receptors = prolonged resistance to Naloxone**)
27
Buprenorphine SE:
- drowsiness, N/V, low abuse risk, ventilation depression, **pulmonary edema**
28
What is buprenorphine's greatest use? - Other uses?
- Opioid use disorder (has low risk of abuse) - Post op, cancer, renal colic (stones), MI, epidurals
29
Which two drugs have resistance to naloxone?
- Buprenorphine and Bremazocine.
30
Which opioid has high incidence of dysphoria and is therefore not utilized clinically?
Nalorphine (σ receptor)
31
Place the following opioid agonist-antagonist in order of potency to Morphine (low to high).
1. Meptazinol 2. Pentazocine 3. Nalorphine = Nalbuphine = Morphine 4. Dezocine 5. Bremazocine 6. Buprenorphine
32
Dezocine: Receptors? CV effects? IM dose? Onset?
- μ δ - No CV effects - 10 -15 mg IM rapid absorption - Onset 15 mins
33
Meptazinol: Receptors? CV effects? IM dose? Onset?
- mu 1 - **lowest affinity** - Duration = 2 hrs - Protein binding: **25%**
34
Which drugs are pure μ-opioid receptor antagonists?
- Naloxone - Naltrexone - Nalmefene
35
**T/F**: All opioid antagonist are competitive -Why is this?
- True - High affinity for all opioid receptors - Bumps the opioid all, binds to receptor, and **inhibits** activation
36
What receptors is naloxone effective on?
- Nonselective μ, κ, δ
37
Naloxone uses (5)
- Neonate (**wdl from mom**) - Hypovolemic/ septic (**↑ CO**) - Antagonism of general anesthesia at high doses (Physostigmine better) - PostOp opioid-induced depression ( must be diluted) - Opioid OD - Detect dependence (abuser would go into wdls after reversal)
38
Naloxone: - Duration of action (DOA)? - Metabolism? - E1/2? - 1st pass? - SE?
- DOA = 30 - 45 mins - Metabolism: **Liver** via glucuronic acid - E1/2 = 60- 90 mins - 1st pass= Hepatic 20% PO - SE: **reversal of analgesia**, **N/V**, ↑ SNS, pulm edema, risk for dysrhythmias (ie: VFib) **push slow 2 - 3 mins**
39
Naloxone Dosages depends on indication: - IV push? - Continuous infusion? - Shock? - Epidural side effects?
- IV: 1-4 mcg/kg - Infusion: 5 mcg/kg b/c DOA - Shock: > 1 mg/kg - 0.25 mcg/kg/hr
40
Which opioid partial agonists have an effect on MAC?
- Pentazocine - Butorphanol - Nalbuphine
41
Naltrexone: - Use - Duration - Most effective route
- Alcoholism - 24 hr duration - PO = most effective
42
Nalmefene: - Potency compared to naloxone What is it's dose, max, & half life?
- Equipotent to naloxone - 15 - 25 mcg IV q 2 - 5 mins (max of 1 mcg/**kg**) - E1/2: 10.8 hrs
43
Methylnaltrexone: - Use - Is it highly ionized or nonionized? How is this clinically significant?
- Promotes gastric emptying and antagonizes N/V - **highly ionized** (**quaternary**): Peripheral pain (CRTZ zone - ↓ N/V ) - **No CNS alteration of analgesia**
44
Alvimopan: - receptor and route? - use - metabolized Long term complications?
- **μ-selective PO peripheral** opioid antagonist for **post-op ileus**. - Metabolism: Gut flora - Long - term CV events
45
Which agonist-antagonist has 50 times greater μ receptor affinity than morphine?
Buprenorphine
46
What are the tamper/abuse-resistant opioid formulations?
- S**ub**ox**one** (**bu**prenorphine + nalox**one**) - E**m**beda (long-release **m**orphine + naltrexone) - OxyNal (**O**xycodone + **N**altrexone)
47
- Which opioids-agonists have a significant effect on volatiles? (Think **RAFS**) - What do they do?
- What do they do?: **Decreases anesthetic requirements (↓ MAC)** - **R**emifentanil: ↓ MAC 50 - 91% - **A**lfentanil: ↓ MAC up to 70% - **F**entanyl: ↓ MAC Isoflurane and Desflurane 50% - **S**ufentanil: ↓ MAC Enflurane 70 - 90% ## Footnote Close CV monitoring. Don't think percentages are important
48
Per lecture, what dose of Fentanyl affects MAC?
- 3 μg/kg IV 25 - 30 min prior to incision
49
- Which opioids-agonist-Antagonist effect volatiles? (Think **BNP**)
- Butorphanol (11%) - Nalbuphine (8%) - Pentazocine (20%)
50
PCA MORPHINE: - Bolus - Basal - Bolus interval
- 1 - 2 mg - 0 - 2 mg/hr - 6 -10 mins
51
PCA Hydromorphone: - Bolus - Basal - Bolus interval
- 0.2 - 0.4 mg - 0 - 0.4 mg/hr - 6 - 10 mins
52
PCA Fentanyl: - Bolus - Basal - Bolus interval
- 20 - 50 **mcg** - 0 - 60 **mcg**/hr - 5 - 10 mins
53
PCA basal rates are not typically recommended for opioid- ____- patients
Naive
54
Ketamine has analgesic effects with doses greater than _____%.
- 50%
55
Where are receptors targeted with opioid neuraxial anesthesia (epidural/spinal)?
- Opioid receptors of the **substantia gelatinosa** (Lamina II). - Used for acute and chronic pain - **No sympathectomy, sensory block, or weakness/motor block**
56
Epidural space is vascular. How do we confirm we are not in epidural vein?
- Aspirate
57
Epidural space is a _____ space.
- Potential
58
How much air can be put into epidural space?
- 3 cc (reabsorbed)
59
What is general rule of dosing for epidural v spinal opioids?
- Dose = 5 - 10 x more than spinal dose
60
Diffusion of opioids across the _____ results in systemic absorption.
dura
61
Epidural uptake includes ___ & ___.
- fat; epidural venous plexus
62
Goal for epidural uptake:
- Opiate or LA (local anesthetic) to diffuse across dura into CSF, bathe spinal cord, and enter dorsal horn (Lamina II)
63
Where can opioids be injected during an epidural that results in systemic absorption? What should be done if this occurs?
- **Epidural venous plexus** - Epinephrine + -caine drug (Epi wash) -keeps drug in epidural space Neo also clinically indicated
64
What is Cephalad movement (in regards to epidurals)?
Cephalad Movement = the movement of drug up the spinal cord towards the brain
65
What drug attribute decreases cephalad movement?
- High Lipid solubility - High to low: Sufentanil >>> Fentanyl >> Morphine
66
________ exhibits much more cephalad movement than __________. Why is this?
- Morphine; Fentanyl/Sufentanil - Why? Fentanyl & Sufentanil are highly lipid soluble = **less** cephalad movement towards brain -Morphine is less lipid-soluble = **more** cephalad movement via CSF bulk flow
67
What factors can cause cephalad movement?
- Coughing/ straining (Valsalva) - Drug baracity - Body position
68
What caution must you take using Valsalva maneuver to induce cephalad movement?
- Risk for unintended high spinal → activates cardiac accelerators → cardiac arrest
69
What is drug baracity?
- Determines how the drug spreads in relation to density - High density: **Hyperbaric** = follows gravity and **sinks** (settles towards dependent area) - Low density: **Hypobaric** = rises against gravity and **floats** towards non-dependent area - Isobaric: remains at level (ie: Abd. procedures)
70
What LA baracity would affect the R hip of a patient positioned on the L lateral side?
- Hypobaracity; Needs to float up to right him
71
When would **epidural CSF levels peak** for the following drugs: - Fentanyl - Sufentanil - Morphine
- Fentanyl - 20 mins - Sufentanil - 6 mins - Morphine - **1 - 4 hrs**
72
Which opioid agonist typically used for walking epidurals in OB?
- Sufentanil
73
When would **epidural administered plasma levels peak** for the following drugs: - Fentanyl - Sufentanil - Morphine
- Fentanyl - 5 - 10 mins - Sufentanil - < 5 mins (crosses dura rapidly) - Morphine - 10 - 15 min
74
When would **intrathecal/cervical** administered **CSF levels peak** for the following drugs: - Fentanyl - Sufentanil - Morphine
- Fentanyl - minimal - Sufentanil - minimal - Morphine - 1 - 5 hours (via CSF bulk flow)
75
If your patient goes apneic during intrathecal dose, which opioid agonist might have caused this? What part of cord is affected?
- Morphine - C3 - C5 (phrenic nerve)
76
Where do we want all spinal anesthetics to go?
- T8 (lower rib cage) per Castillo
77
What is T1 - T4?
- Cardiac accelerators
78
Anatomical point of T4?
- Nip line
79
If given spinal with Lido, what CV effects do you expect to see? - What can you do pre-op to help prevent this?
- Decrease BP Increase HR - 500 cc - 1 L bolus - goal SBP > 140 typically
80
What is the most common side effect from neuraxial opioid administration? Why does this occur?
- **Pruritus** - face, neck, upper chest - Cephalad migration to **trigeminal nucleus** - Prevalent in OB, elderly
81
What are the treatments for neuraxial- induced pruritus? (Think **PANG**)
- **Naloxone** 0.25 mcg/kg/hr IV) - Antihistamines -Gabapentin - Propofol 10 - 20 mg (GABA-a; risk for loss of airway reflexes)
82
Other SE: - CNS - Pulmonary - GI/GU: - Viral: - Fetal:
- CNS: Sedation :) , Skeletal muscle rigidity; sz-like (rare) - Pulmonary: Resp depression - GI: N/V - GU: Urine retention (males; sacral interaction affects PNS outflow) - Viral: Herpes virus reactivation - Fetal: Neonatal Morbidity (**No breastfeeding for 24 hrs**)
83
What sign would indicate respiratory depression from neuraxial opioid administration? What is the treatment?
- ↓LOC from ↑CO₂ (hypercarbia) - Early: w/in 2 hrs; Late: 6 - 12 hrs post - Naloxone 0.25 μg/kg/hr IV
84
If neuraxial opioids induced a reemergence of a herpes virus, how long would this occur after opioid administration?
- 2 - 5 days after epidural opioid
85
Other words for spinal neuraxial opioid block:
- Intrathecal, Subarachnoid

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