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Anesthesia Pharmacology > Exam 1 - Benzodiazepines > Flashcards

Exam 1 - Benzodiazepines Flashcards

1
Q

How do anesthetics mimic sleep?

A
  • Inhibits thalmic and mid-brain RAS
  • Reversibly inhibit CNS
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2
Q

What is important to remember about reported cases of awareness?

A

Important to know what anesthetic they were given (twighlight sedation?)
Many include induction and emergence as awareness

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3
Q

How did we come to use EEG to determine anesthetic depth?

A
  • EEG activity is related to CBF and CMRO2
  • Anesthetics alter CBF and CMRO2
    Therefore we can use EEG to estimate anesthetic depth
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4
Q

What drugs can decrease BIS?

A

Synergistic anesthetics like hypnotics, volatiles, NMB, opiods

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5
Q

What range of BIS prevents recall?

A

40-60

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6
Q

What should the EMG be on a paralyzed patient?

A

0

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7
Q

What is the supression ratio?
What should it be?

A
  • Measures how often the patient’s BIS hit 0
  • Should never have a number here or your anestheic is way too deep
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8
Q

How do sympathomimetics and sympatholytics affect the BIS?

A
  • Sympathomimetics: may have a ↑ BIS due to ↑ catecholamines, but are still amnestic (ketamine)
  • Sympatholytics: BIS may be lower due to decreased SNS activity, despite having actually being more aware
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9
Q

What are the 5 effects of benzodiazepines?

A
  1. Anxiolysis
  2. Sedation
  3. Anterograde amnesia (lasts longer than sedation)
  4. Anticonvulsant
  5. Spinal cord mediated muscle relaxation
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10
Q

What is the MOA of benzodiazepines?

A
  • Binds to GABA A⍺/Ɣ subunits increasing Cl- entry into the cell causing hyperpolarization
  • Potentiates the GABA site
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11
Q

What are benzos different effects at ⍺1 and ⍺2 subunits?

A
  • ⍺1: sedative, amnestic, anticonvulsant (most abundant)
  • ⍺2: anxiolytic, skeletal muscle
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12
Q

What other drugs bind at the GABAA site?

A
  • Barbituates
  • Etomidate
  • Propofol
  • Alcohol
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13
Q

What is the distrubution of benzos?

A
  • Highly lipid soluble
  • Highly protein bound to albumin
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14
Q

What drug interactions do you need to worry about with benzos?

A
  • Drugs that cause synergestic effects: alcohol, LA, opiods, ⍺2 agonists, volatiles
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15
Q

What effect may benzos have on clotting?

A

BZD inhibit platelet aggregating factor causing a conformational change in the membrane… unclear if clinically significant

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16
Q

What does the pH of versed change about its solubility?

A

pH < 3.5 imidazole ring is open = protonated and water soluble (inactive)
pH > 4.0 = imidazole ring is closed = lipid soluble and unprotonated (active)

pH is 3.5 in solution

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17
Q

What is the onset, peak, half life, and duration of midazolam?

A

Onset: 1-2 mins
Peak: 5 mins
1/2 time: 2 hours
Duration: short due to rapid distrubution to tissues

18
Q

How is midzolam metabolized?
What are its metabolites?

A
  • CYP3A4
  • Active: 1-hydroxymidazolam (1/2 activity of parent)
19
Q

What drugs inhibit P450 enzymes?

A

Cimetidine
Erythromycin
Calcium channel blockers
Antifungal
Fentanyl

20
Q

What are the neurological effects of midazolam?

A
  • ↓CBF/CMRO2
  • Has EEG ceiling effect, unable to produce isoelectric EEG
  • Preserves CO2 vasomotor response
  • No change in ICP
21
Q

What are the pulmonary effects of midazolam?

A
  • Dose dependent decrease in ventilation
  • Depresses swallowing reflex and upper airway activity = aspiration risk
22
Q

What are the CV effects of midazolam?

A

↑ HR, ↓BP, ↓SVR
CO unchanged

23
Q

What is the preop dosing for midazolam for children and adults?

A

Children: 0.25-0.5mg/kg orally
Adults: 1-5mg IV

24
Q

What is the efficacy of midazolam in children?

A

Midazolam is very safe even at higher does.
Does not prolong emergence or recovery time.

25
Q

What is the induction dose for midazolam?

A

0.1-0.2 mg/kg over 30 seconds

26
Q

Why is versed bad for postoperative sedation?

A

Awakening is markedly delayed d/t accumulation of active metabolites in tissues

27
Q

Why does valium burn on injection?

A

The solvent propylene glycol

28
Q

What is the onset, peak, half time, and duration of diazepam?

A

Onset: 1-5 mins
Peak: 1 hour
Half time: 20-40 hours
Duration: Longer than versed, shorter than ativan

29
Q

How is diazepam metabolized?
Active metabolites?

A
  • CYP3A
  • Desmethyldiazepam (48-96hrs) and oxazepam
30
Q

What are the CNS effects of diazepam?

A
  • ↓CBF/CMRO2
  • Potent anticonvulsant
  • Can produce an isoelectric EEG
31
Q

What are the pulmonary effects of diazepam?

A
  • Minimal effects on ventilation but can be worsened by opioiods, EtOH, and COPD
  • Depressant effects reversed by painful stimuli
32
Q

What are the CV effects of diazepam?

A
  • Minimal effects on BP, HR, and SVR
  • BP can be dropped with addition of opioids
33
Q

What are the neuromuscular effects of valium?

A

Decreases skeletal muscle tone

34
Q

What is the induction dose for valium?

A

0.5-1.0 mg/kg IV

35
Q

Of the 3 benzos in lecture, which one is the most potent amnestic and sedative?

A

Ativan (lorazepam)

36
Q

Why does lorazepam have a slower onset of action?

A

Less lipid soluble, takes longer to reach CNS

37
Q

What is the peak, half-time, and metabolism of lorazepam?

A

Peak: 20-30 mins
Half-time: 14 hours
Metabolism: Direct conjugation (better for liver dx)

38
Q

What is the bolus dose for ativan?

A

1-4 mg

39
Q

What drugs do flumazenil reverse?

A

Any drug that agoinizes the benzodiazepine receptor - including psych meds

40
Q

What is the dosing for Romazicon?

A

0.2 mg IV then 0.1 mg q 1 min, up to 1 mg total

41
Q

What is important to know about Romazicons duration of action?

A

Duration = 30-60 mins; may need to be redosed if the sedative duration is longer than that

42
Q

When is flumazenil contraindicated?

A

Antiepileptic drugs

Anesthesia Pharmacology (5 decks)

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