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
  1. Hypnotics
  2. volatiles
  3. NMBs
  4. opioids
  5. 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

< 3.5 pH = water soluble, protonated (ring open) (inactive form)
>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
Versed Vd
Large (1000ml-1500ml/kg)
26
Versed metabolism
CYP3A4 (hepatic Microsomal enzymes)
27
Significant Drugs that can decrease BZD metabolism by CYP inhibition (FACCE)
* Fentanyl * Antifungals * Cimetidine, CCBs * Erythromycin
28
Versed cerebral flow effects
Decrease CMRO2. Decrease CBF. (Both dose related)
29
Versed CNS effects (2)
- Potential anticonvulsant - Unable to produce isoelectric EEG (flatline)
30
Versed CO2 cerebral flow effects
High CO2 = cerebral vasodilation Low CO2 = cerebral vasoconstriction Versed preserves CO2 vasomotor response
31
Versed ICP effects
No effect on ICP (neuro-safe)
32
Versed pulmonary effects
Dose dependent decrease in ventilation
33
Versed airway effects
Depresses swallow reflex and upper airway activity increased risk of aspiration
34
Versed CV effects
Dose dependent increase HR and decreased BP (CO unchanged d/t compensation)
35
Versed sedation/anxiolysis dosing (adult)
1-5 mg IV. Peaks 5 min
36
Versed sedation/anxiolysis children dose
0.25-0.5 mg/kg oral. Peak 20-30 min
37
Versed induction dose
Not common as induction. 0.1-0.2 mg/kg IV over 30-60 sec followed by fentanyl 50-100 mcg
38
Versed Postoperative sedation dose
1-7 mg/hr IV Not recommended for use more than 2-3 days d/t immune/T cell effects
39
Diazepam trade name
Valium
40
Valium protein binding
Highly protein bound
41
Valium duration (comp)
More prolonged duration than versed. Rarely used in anesthesia.
42
Valium solubility
Insoluble in water Need propylene glycol = pain on injection
43
Valium onset and duration (comp)
Onset: 1-5 minutes. Duration longer than versed.
44
Valium E 1/2 time
20-40 hours.
45
Valium metabolism
CYP3A Active metabolite nearly as potent (48-96 hr) return of drowsiness 6-8 hrs
46
Valium cerebral flow effects
Dose related decrease in CMRO2 and CBF.
47
Valium anticonvulsant dose
0.1 mg/kg IV.
48
Valium EEG effects
Can produce isoelectric EEG (flatline).
49
Valium pulmonary effects
Minimal effects on ventilation.
50
Valium CV effects
Minimal decrease in BP, CO, and SVR.
51
Valium induction dose
0.5-1 mg/kg IV Decrease 25-50% in: elderly, liver disease, presence of opioids
52
Valium neuromuscular effects
Skeletal muscle relaxant (not paraytic) tolerence develops over time
53
Lorazepam trade name
Ativan
54
Ativan potency (comp)
More potent compared to other BZDs.
55
Ativan solubility
Insoluble in water Requires polyethylene glycol = burns on injection
56
Ativan onset (comp) and peak
Slower onset than versed and Valium Peak: 20-30 min with 1-4mg IV dose
57
Ativan E 1/2 time
14 hours.
58
Ativan metabolism
Conjugated to inactive metabolites Less dependent on hepatic enzymes
59
Ativan dose
1-4 mg IV.
60
Flumazenil trade name
Romazicon.
61
Flumazenil MOA
Competitive antagonist for BZD receptor.
62
Flumazenil metabolism
Hepatic Microsomal enzymes.
63
Flumazenil dose
0.2 mg IV Repeat 0.1 mg q1 min max 1 mg total to consciousness
64
Flumazenil duration
30-60 min (shorter than BZD => resedation from BZD).
65
Flumazenil side effects
No significant side effects.
66
Flumazenil contraindication
Contraindicated in pt taking antiepileptic drugs.