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TxWes Spring '25: Anesthesia Pharm > Benzodiazepines Exam 1 > Flashcards

Benzodiazepines Exam 1 Flashcards

1
Q

Sedative/hypnotics definition

A

Drug that induces sleep, calm or hypnosis

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2
Q

How is EEG monitoring used to measure drug effects?

A

Anesthesia alters CBF and CMRO2.
CBF and CMRO2 relate to EEG activity.

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3
Q

What is BIS monitoring?

A

Processed EEG compacted into one waveform.
Helps determine level of sedation/consciousness.
BIS 100 = awake
BIS 0 = coma

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4
Q

What number on the BIS indicates loss of consciousness?

A

BIS < 58

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5
Q

BIS < 65 indicates…

A

<5% chance of consciousness within 50 seconds

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6
Q

SQI on BIS monitor

A

Signal quality index. Measures quality or lack of interference.

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7
Q

SR on BIS monitor

A

Suppression Ratio.
Percentage of time that the EEG signal is suppressed or flat
***anesthesia should not see a SR of zero (indicates oversedation or brain death)

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8
Q

Examples of BIS suppressants (5)

A

Hypnotics, volatiles, NMBD, opioids, beta blockers

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9
Q

Examples of BIS stimulants (2)

A

Ketamine, Epinephrine

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10
Q

Ideal range for BIS under general anesthesia

A

40-60

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11
Q

Pharmacologic effects of BZDs (5)

A
  • Anxiolytic
  • Sedation
  • Anterograde amnesia (forward)
  • Anticonvulsant
  • Skeletal muscle relaxation (not paralysis)
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12
Q

BZD benefit over barbiturates (3)

A
  • Less tolerance or abuse potential
  • Fewer/less severe side effects
  • Don’t induce CYP450
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13
Q

BZD MOA

A

Enhances effects of GABA on GABA-A receptors
enhanced open of chloride channels
hyperpolarization of neuron, less firing

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14
Q

GABA alpha-1 effects (3)

A
  • Sedative
  • Amnesia
  • Anticonvulsant
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15
Q

GABA alpha-2 effects (2)

A
  • Anxiolytic
  • Skeletal muscle relaxation
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16
Q

Synergistic drugs also acting on GABA-A (4)

A

Barbiturates, Etomidate, Propofol, Alcohol

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17
Q

BZD EEG effects (2)

A
  • Decrease alpha wave activity, relaxation
  • Some able to flatten brain waves
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18
Q

Midazolam trade name

A

Versed

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19
Q

Versed amnesia vs sedation effects

A

Amnestic effects last longer than sedation effects

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20
Q

Versed solubility with pH

A

In less than 3.5 pH => water soluble, protonated (ring open) (inactive form)
In more than 4 pH => lipid soluble, unprotonated (ring closed) (active form)

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21
Q

Versed onset and peak effect

A

Onset: 1-2 min
Peak: 5 min

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22
Q

Versed protein binding

A

Extensively bound 96-98%

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23
Q

BZD reversal drug

A

Flumazenil (Romazicon)

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24
Q

Versed E 1/2 time

A

2 hours. Doubled in elderly pts.

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25
Q

Versed Vd

A

Large (1000ml-1500ml/kg)

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26
Q

Versed metabolism

A

CYP3A4 (hepatic Microsomal enzymes)

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27
Q

Significant Drugs that can decrease BZD metabolism by CYP inhibition (3)

A

Cimetidine (Tagamet)
erythromycin
Calcium channel blockers
antifungals
Fentanyl

28
Q

Versed cerebral flow effects

A

Decrease CMRO2. Decrease CBF. (Both dose related)

29
Q

Versed EEG effects

A
  • Potential anticonvulsant
  • Unable to produce isoelectric EEG (flatline)
30
Q

Versed CO2 cerebral flow effects

A

High CO2 = cerebral vasodilation
Low CO2 = cerebral vasoconstriction
Versed preserves CO2 vasomotor response

31
Q

Versed ICP effects

A

No effect on ICP (neuro-safe)

32
Q

Versed pulmonary effects

A

Dose dependent decrease in ventilation

33
Q

Versed airway effects

A

Depresses swallow reflex and upper airway activity
increased risk of aspiration

34
Q

Versed CV effects

A

Dose dependent increase HR and decreased BP
(CO unchanged d/t compensation)

35
Q

Versed sedation/anxiolysis dosing (adult)

A

1-5 mg IV. Peaks 5 min

36
Q

Versed sedation/anxiolysis children dose

A

0.25-0.5 mg/kg oral. Peak 20-30 min

37
Q

Versed induction dose

A

Not common as induction.
0.1-0.2 mg/kg IV over 30-60 sec
followed by fentanyl 50-100 mcg

38
Q

Versed Postoperative sedation dose

A

1-7 mg/hr IV
Not recommended for use more than 2-3 days d/t immune/T cell effects

39
Q

Diazepam trade name

A

Valium

40
Q

Valium protein binding

A

Highly protein bound

41
Q

Valium duration (comp)

A

More prolonged duration than versed. Rarely used in anesthesia.

42
Q

Valium solubility

A

Insoluble in water
Need propylene glycol = pain on injection

43
Q

Valium onset and duration (comp)

A

Onset: 1-5 minutes. Duration longer than versed.

44
Q

Valium E 1/2 time

A

20-40 hours.

45
Q

Valium metabolism

A

CYP3A
Active metabolite nearly as potent (48-96 hr)
return of drowsiness 6-8 hrs

46
Q

Valium cerebral flow effects

A

Dose related decrease in CMRO2 and CBF.

47
Q

Valium anticonvulsant dose

A

0.1 mg/kg IV.

48
Q

Valium EEG effects

A

Can produce isoelectric EEG (flatline).

49
Q

Valium pulmonary effects

A

Minimal effects on ventilation.

50
Q

Valium CV effects

A

Minimal decrease in BP, CO, and SVR.

51
Q

Valium induction dose

A

0.5-1 mg/kg IV
Decrease 25-50% in: elderly, liver disease, presence of opioids

52
Q

Valium neuromuscular effects

A

Skeletal muscle relaxant (not paraytic)
tolerence develops over time

53
Q

Lorazepam trade name

A

Ativan

54
Q

Ativan potency (comp)

A

More potent compared to other BZDs.

55
Q

Ativan solubility

A

Insoluble in water
Requires polyethylene glycol = burns on injection

56
Q

Ativan onset (comp) and peak

A

Slower onset than versed and Valium
Peak: 20-30 min with 1-4mg IV dose

57
Q

Ativan E 1/2 time

A

14 hours.

58
Q

Ativan metabolism

A

Conjugated to inactive metabolites
Less dependent on hepatic enzymes

59
Q

Ativan dose

A

1-4 mg IV.

60
Q

Flumazenil trade name

A

Romazicon.

61
Q

Flumazenil MOA

A

Competitive antagonist for BZD receptor.

62
Q

Flumazenil metabolism

A

Hepatic Microsomal enzymes.

63
Q

Flumazenil dose

A

0.2 mg IV
Repeat 0.1 mg q1 min
max 1 mg total to consciousness

64
Q

Flumazenil duration

A

30-60 min (shorter than BZD => resedation from BZD).

65
Q

Flumazenil side effects

A

No significant side effects.

66
Q

Flumazenil contraindication

A

Contraindicated in pt taking antiepileptic drugs.

TxWes Spring '25: Anesthesia Pharm (8 decks)

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