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Anesthesia Pharmacology > Exam 2 - Opioid Agonist-Antagonists and Antagonists > Flashcards

Exam 2 - Opioid Agonist-Antagonists and Antagonists Flashcards

1
Q

What are the advantages of using opioid agonist-antagonists?

A
  • Analgesia
  • Limited ventilatory depression
  • Low potential for physical dependence
  • Ceiling effect prevents additional responses
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2
Q

Explain the ceiling effect?

A
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3
Q

What is pentazocine’s MOA?

A

Agoinst effects on delta and kappa receptors with weak antagonist activity

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4
Q

Pentazocine is antagonized by ____
____ as potent as nalorphine
Extensive ____
Excreted as ____ in the urine

A
  • naloxone
  • 1/5th
  • hepatic first pass
  • glucoronide conjugates
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5
Q

What is pentazocine used for and at what dose? (IV, IM, PO)

A

Moderate chronic pain
IV: 10-30mg
IM: 20-30mg
PO: 50mg

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6
Q

Why do we like Pentazocine for epidural analgesia?

A

Bc it has shorter duration than morphine

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7
Q

Pentazocine s/e are similar to morphine’s.
What can it cause at high doses?
What cardiac effects do you see?

A

Dysphoria
CV: ⬆in HR, BP, pulmonary artery BP, LVEDP

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8
Q

What must you consider when giving Pentazocine to pregnant women?

A

It crosses the placental barrier and can cause fetal depression

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9
Q

Is Butorphanol more potent than pentazocine? (Agonist and Antagonist effects)

A

Yes
Agonist: 20x >
Antagonist: 10-30x >

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10
Q

How does butorphanol produce analgesia and anti-shivering effects?

A

Moderate affinity for kappa receptors

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11
Q

Dosing for butorphanol?
Equivalent to how many mg of morphine?

A
  • 2-3 mg IM
  • 10 mg morphine
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12
Q

It may be difficult to use another ____ in the prescence of butorphanol?

A

Opioid agonist

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13
Q

What are the generalized side effects of Opioid Agonist-Antagonists?

A

They are the same as opioid agonists + dysphoric reactions.

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14
Q

Nalbuphine is a ____ receptor agonist and is equally potent to ____

A

Mu
Morphine

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15
Q

Which agonist antagonist opioid is good to use in patients with cardiovascular dz?

A
  • Nalbuphine
  • It does not cause an increase in BP, pulm pressures, HR, or atrial pressures
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16
Q

Buprenorphine is a ____ receptor agoinst with an affinity ____ than morphine

Why can this be a problem?

A
  • Mu
  • 50x greater
  • Has a prolonged resistance to naloxone
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17
Q

How much buprenorphine is equal to 10 mg of morphine?

A

0.3 mg IM

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18
Q

Nalorphine is not used as clinically because of?
What is its morphine potency?

A
  • High incidence of dysphoria with sigma receptor activation
  • Equivalent potency to morphine
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19
Q

Bremazocine has a receptor affinity for ____ receptors that is ____ more potent than morphine
Can it be reversed by naloxone?

A
  • Kappa
  • 2x
  • No
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20
Q

Similar to Nalbuphine, in that they both do not exhibit cardiovascular effects.

A

Dezocine

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21
Q

Dezocine IM dose?

A

10 - 15 mg IM or 0.15 mg/kg IM

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22
Q

100 mg of Meptazinol is = to ____ mg of morphine
What receptor does it work on?

A
  • 100 mg Meptazinol = 8 mg morphine
  • Mu 1
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23
Q

What is the MOA of opioid antagonists?

A

Pure mu opiod competitive antagonist with no agonist activity

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24
Q

This opioid antagonist is nonselective for all 3 opioid receptors?

A

Naloxone

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25
What are the uses for naloxone?
- Post op opiod induced depression - Neonate, from mom - Opiod OD - Detecting dependence - Hypovolemic/septic shock (increases myocardial contractility) - Antagonizes general anesthesia in high doses
26
Naloxone dosing IV: Continuous infusion: Shock: Epidural side effects:
IV: 1-4 mcg/kg Continuous infusion: 5 mcg/kg Shock: >1 mg/kg Epidural side effects: 0.25 mcg/kg/hr
27
How long does naloxone last?
30-45 mins (may need to redose)
28
Side effects of naloxone?
- Reversal of analgesia - N/V - Increased SNS
29
What opioid antagonist works better PO? Uses?
- Naltrexone - Alcoholism
30
What is the dose for Nalmefene?
15 to 25 mcg IV (q 2 to 5 minutes) OR 1 mcg/kg
31
Nalmefene is equipotent to...
Naloxone
32
Nalmefene has a half time of?
10.8 hours
33
Is Methylnaltrexone ionized or nonionized?
Highly ionized
34
Methylnaltrexone uses?
- Promotes gastirc emptyinh and antagonizes N/V - No alteration in centrally mediated analgesia
35
What is the newer, mu-selective PO peripheral opioid antagonist that is used mainly for post-op ileus?
Alvimopan
36
Where is Alvimopan metabolized?
Gut Flora
37
What is a risk of using Alvimopan long term?
Adverse CV Events
38
What are the three tamper/abuse-resistant opioids discussed in class?
Suboxone Embeda OxyNal
39
Buprenorphine plus naloxone...
Suboxone
40
Extended release morphine plus naltrexone...
Embeda
41
Oxycodone plus naltrexone...
OxyNal
42
Are allergies to opioids true allergies?
- Not really, only 3 documented cases - S/E are due to histamine release, orthostatic hypotension, N/V
43
What can prolonged exposure to opioids and abrupt withdrawl cause?
- Immunosuppression
44
What is given that decreases MAC of Iso or Desflurane to 50%?
Fentanyl 3mcg/kg IV 25-30 minutes before surgical incision
45
What are the effects on MAC with the following opioid agonists? Sufentanil Alfentanil Remifentanil
Sufentanil decreases MAC with Enflurane by 70-90% Alfentanil can decrease MAC up to 70% Remifentanil can have a 50-91% decrease in MAC
46
Which opiod agonist-antagonists can decrease MAC?
- Butorphanol - Nalbuphine - Pentazocine
47
What are the Patient-Controlled Analgesia doses for: Morphine Hydromorphone Fentanyl
48
Why is PCA sometimes better than prn dosing?
49
Benefits of neuraxial opioids?
- No sympathectomy, sensory block, or weakness
50
What is the dose change for epidurals compared to spinals?
5x-10x the dose, has to diffuse accross the dura
51
What opioids are given in an epidural and there action? (include peak csf times)
**Fentanyl** - highly lipophilic (800x more than morphine) - peaks in 20 mins **Sufentanil**: highly lipophilic (1600x morphine) - peaks in. 6 mins **Morphine**: Slower onset but longer duration - peaks in 1-4 hours
52
What is the pathway for drugs for epidural uptake?
- Epidural fat → epidural venous plexus → systemic absorption → diffusion across dura → CSF
53
What can you do to help reduce systemic absoption of epidural opioids?
Add a vasoconstrictor
54
What contributes to cephalad movement of spinal opioids?
- Lipid solubility - Coughing or straining
55
Which drugs tend to have cephalad movements more when given intrathecally?
Morphine > fentanyl and sufentanil Morphine remains in the CSF more and can migrate upwards, whereas fentanyl crosses into the spinal cord
56
What are hypobaric and hyperbaric drugs?
Hypobaric drugs float in solution Hyperbaric drugs are more dense and sink in solution Positioning affects drug migration due to gravity
57
Plasma peak of epidural fentanyl, sufentanil, and morphine?
Fentanyl: 5-10 min Sufentanil: < 5 min Morphine: 10 - 25 min
58
Cervical CSF peak levels of fentanyl, sufentanil, and morphine?
Fentanyl: minimal Sufentanil: minimal Morphine: 1-5 hours
59
Most common side effect of neuraxial opiods? Cause? Tx?
- Pruritis - Cephalad migration to trigeminal nucleus - Tx: naloxone, antihistamines, gabapentin
60
Who is at high risk for urinary retention d/t neuraxial opioids?
Males, due to interaction at the sacral spinal cord inhibiting PNS outflow
61
What is the most reliable sign of depression of ventilation d/t neuraxial opiods? Tx?
- Depressed LOC d/t hypercarbia - Naloxone 0.25 mcg/kg/hour to decrease side effects
62
What can be reactivated 2-5 days after epidural opioid administration?
Herpes simplex labialis

Anesthesia Pharmacology (23 decks)

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