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Spr24 Pharm II > Opioid agonists pt 2 (Ex2) > Flashcards

Opioid agonists pt 2 (Ex2) Flashcards

1
Q

How potent is fentanyl?

A
  • 75 - 125 x morphine.
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2
Q

What is the blood-brain equilibration of fentanyl?
What does this mean?

A
  • 6.4 minutes
  • Potent with rapid onset and ↑ lipid solubility.
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3
Q

What percent of fentanyl is subject to lung first-pass effect?
What does this mean?

A
  • 75%
  • Drug is taken up into lung tissue and possibly subjected to breakdown via pulmonary esterases.
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4
Q

Where is fentanyl metabolized?
What is its principal metabolite?

A
  • Liver via CYP3A
  • Norfentanil
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5
Q

How does fentanyl dosing change for the elderly or liver cirrhosis?

A

No change in elderly or cirrhotic patients.

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6
Q

Describe what the graph below is showing.

A

Fentanyl has the greatest context-sensitive half-time of any of the fentanyl derivatives.

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7
Q

What is the analgesia dosage of fentanyl?
Induction dose?

A
  • Analgesia: 1 - 2 μg/kg IV
  • Induction: 1.5 - 3 μg/kg IV
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8
Q

1mg of PO fentanyl = ____ mg of IV morphine

A

5

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9
Q

What is the intrathecal dosage of fentanyl?

A

25 mcg

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10
Q

What is the adult oral dose of fentanyl?
Pediatric?

A
  • Adult: 5 - 20 mcg/kg
  • Peds: 15 - 20 mcg/kg
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11
Q

What is the transdermal dose of fentanyl?

A
  • 75 - 100 μg (18 hours steady delivery)
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12
Q

What cardiovascular side effects should be known about fentanyl?
What CNS side effects should be known?

A
  • ↓BP & ↓CO
  • Can cause seizures & modestly increase ICP.
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13
Q

How much more potent is sufentanil than fentanyl?

A
  • 5-12 times more potent.
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14
Q

How much of sufentanil is subject to first pass effects?

A
  • 60% lung first-pass
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15
Q

How much of sufentanil is protein bound? What protein is it bound to?

A

92.5% α-1 acid glycoprotein bound.

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16
Q

What is the analgesia dose of sufentanil?

A
  • Analgesia: 0.1 - 0.4 μg/kg IV
17
Q

What is the induction dose of sufentanil?

A

18.9 mcg/kg IV

18
Q

What is the potency of alfentanil?
What is its onset?

A
  • 20% as potent as fentanyl
  • Onset: 1.4 min (faster than all derivatives except remifentanil)
19
Q

What is the alfentanil induction dose?
What about laryngoscopy dose?
What about maintenance?

A
  • Induction: 150 - 300 μg/kg IV
  • Laryngoscopy: 15 - 30 μg/kg IV
  • Maintenance: 25 - 150 μg/kg/hr IV with inhaled anesthetics
20
Q

What drug can cause acute dystonia when given to a Parkinson’s patient?

A

Alfentanil

21
Q

What receptor affinity does remifentanil have?
How potent is it?

A

selective μ opioid agonist
same potency as fentanyl

22
Q

What is remifentanil’s structure and why is it important?

A

Ester Structure = hydrolyzed by plasma & tissue esterases.

  • Rapid onset & offset
  • Very titratable
  • No accumulation
23
Q

Answer the following characteristics of remifentanil below:
Clearance:
Peak effect:

A
  • Clearance: 3-4L/min (8x faster than alfentanil)
  • Peak: 30-60 seconds (fastest fentanyl derivative)
24
Q

What is the induction dose of remifentanil?

A
  • 1 μg/kg IV over 1 min
25
Q

What is the maintenance dosing of remifentanil?

A
  • 0.005 - 2 μg/kg/min IV
26
Q

How potent is hydromorphone?
What dose should be given?
What benefits does hydromorphone have over morphine?

A
  • 5x more potent than morphine
  • 0.5mg IV → 1-4 mg total
  • No histamine release & no active metabolites.
27
Q

Why is codeine not given IV?

A
  • Induced hypotension via histamine release.
28
Q

What is the dose of codeine for cough suppression?
Analgesia?

A
  • Cough: 15mg
  • Analgesia: 60mg (= about 5mg morphine)
29
Q

Which opioid is most cleared?

A
  • Remifentanil (3-4L/min)
30
Q

Which opioid(s) is/are the most protein bound?
Which is the least?

A
  • Sufentanil, alfentanil, & remifentanil
  • Least = morphine
31
Q

Which opioid is the highest percent non-ionized?

A
  • Alfentanil
32
Q

Morphine tends to relieve _____ type pain more than _____ type pain.

A

Dull: sharp

33
Q

Opioid + N2O or benzos can lead to?

A

CV depression (CO & BP)

34
Q

What negative effect does post-op shivering have?

A

increased metabolic demand 500%

35
Q

What is the sufentanil intraop dose?
What is the infusion dose?

A

intraop: 0.3 - 1μg/kg IV
infusion: 0.5 - 1μg/kg/hr IV

36
Q

What is the metabolism profile for alfentanil? (metabolized by and metabolite)

A

metabolized by hepatic p450
metabolite: noralfentanil

37
Q

What is the E1/2 time of remifentanil?

A

6.3 minutes

38
Q

How potent is tramadol?

A

5-10x less than morphine

Spr24 Pharm II (32 decks)

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