Exam 1 - Benzos Flashcards

(49 cards)

1
Q

What is Sedation?

A

Drug that induces calm or sleep

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2
Q

What is Hypnotics

A

Drug that induces hypnosis or sleep

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3
Q

What BIS score is considered unconscious?

A

<58

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4
Q

What is a normal range for BIS?

A

40-60

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5
Q

What BIS # should never have a value?

A

SR; Suppression Ratio

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6
Q

What are the 5 Pharmacologic Effects of Benzos?

A
  1. Anxiolytics
  2. Sedation
  3. Anterograde Amnesia
  4. Anticonvulsant
  5. Spinal-Cord Mediated Skeletal Muscle Relaxation
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7
Q

What is the MOA of Benzos?

A

Enhances the affinity of receptor for GABA at GABAa
- Hyperpolarized Cl- ion channel

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8
Q

What are 2 subunits of GABA?

A

GABA a and GABA y

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9
Q

What is Alpha-1 GABA?
*Location
*Common or not common?

A

Sedative, amnestic, anticonvulsant
*Cerebral Cortex, Cerebellar Cortex, Thalamus
*Most abundant type

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10
Q

What is Alpha-2 GABA?
*Location

A

Anxiolytic, Skeletal Muscle
*Hippocampus, amygdala

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11
Q

What 4 other Drugs bind to GABA-a, making a synergistic effect and increased risk of OD

A

Barbs, Etomidate, Prop, Alcohol

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12
Q

Name 5 Synergistic Drug Interactions to Benzos

A

Alcohol, Injected Anesthetics, Opiates, A2-Agonists, Volatile Anesthetics

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13
Q

True or false: Benzos can inhibit platelet aggregation?

A

True; not clinically significant

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14
Q

What type of ring is Versed?
*When is it open? Protonated vs un? Water or lipid soluble?
*When is it closed? Protonated vs un? Water or lipid soluble?

A

Imidazole ring - stabilizes and allows rapid metabolism
*<3.5, ring is open - protonated - Water soluble
*>4.0 ring is closed - unprotonated - Lipid Soluble

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15
Q

True or False: Versed requires Propylene glycol to stabilize?

A

False

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16
Q

Versed: Onset, peak, E 1/2, and Vd

A

Onset - 1-2 min IV
Peak - 5 min
E 1/2 - 2 hours; x2 in elderly/liver pts
Vd - 1-1.5 L/kg (large); GREATER in elderly and obese pts

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17
Q

Which enzyme metabolizes Versed?
*What is the active metabolite?

A

CYP3A4
*1-hydroxymidazolam

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18
Q

What are 5 Drugs that inhibit CYP450, decreasing metabolism and delaying 1/2 life?

A

Cimetidine, Erythromycin, CCB, Antifungal, Fent

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19
Q

Versed has a _ x CL faster than Lorazepam and _ x CL faster than Diazepam?

A

5x faster than Lorazepam; 10x Faster than Diazepam

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20
Q

Versed CNS Effects: CMRO2, CBF
*Isoelectric EEG
*Vasomotor Response?
*Change in ICP?

A

Decreased CMRO2, CBF [dose related]
*NO Isoelectric EEG - ceiling effect
*Preserves vasomotor response, so increased CO2 will cause vessels to dilate
*No change in ICP, so safe in neuro pts

21
Q

Versed Pulmonary Effects:
*Ventilation
*Swallowing Reflex and Upper Airway Activity

A

*Dose-Dependent Ventilation
*Decreased swallowing reflex and upper airway activity, so aspiration risk

22
Q

Versed CV Effects:
*HR, BP, SVR, CO

A

Increased HR, Decreased BP, Decreased SVR, Maintained CO

23
Q

Versed Sedation Dosing:
*Children w/ Peak time
*Adults w/ Peak time [elderly?]

A

*Children: 0.25-0.50 mg/kg oral
- Peak: 20-30 min
*Adults: 1-5 mg IV; decreased dose in elderly
- Peak: 5 min

24
Q

Versed Induction Dosing:
*What Opiate to give w/ and time?

A

0.1-0.2 mg/kg IV over 30-60 sec
*Fent 50-100 mcg 1-3 min prior

25
Versed Maintenance Dosing:
Uncommon
26
Versed Postoperative Sedation Dosing: *Significance of 2-3 Gtt maintenance
Dose: 1-7 mg/hr IV *T-Cell Suppression
27
Is Versed more Water or Lipid Soluble?
Water Soluble
28
Is Diazepam more Water or Lipid Soluble?
Highly Lipid Soluble
29
True or False: Diazepam is insoluble in water, so it must be mixed with Propylene Glycol?
True
30
Diazepam: Onset, Peak, E 1/2 time
onset: 1-5 min Peak: Peds - 15-30 min; Adults - 1 Hr E 1/2 Time: 20-40 hours
31
Diazepam Metabolism: *Active Metabolites
CYP3A *Desmethyldiazepam and Oxazepam
32
Diazepam CNS Effects: CMRO2 and CBF *Anticonvulsant Dose *Isoelectric EEG
Decreased CMRO2 and CBF *Anticonvulsant - 0.1 mg/kg IV *CAN PRODUCE ISOELECTRIC EEG
33
Diazepam Respiratory Effects: *Ventilation *How to reverse Respiratory Depression
Minimal effect on ventilation *Surgical stimulation
34
Diazepam CV Effects: *BP, CO, SVR *Change in BP is due to....
Minimal decreases in BP, CO, SVR *BP changes due to synergistic effect with opiates
35
Diazepam Neuromuscular Effects: *Skeletal muscle tone *Tolerance?
Skeletal muscle tone decreased and can develop a tolerance
36
Valium Induction Dosing: *Elderly, Liver, Opiates?
0.5-1.0 mg/kg IV *Decreased by 25-50%
37
True or False: Lorazepam is insoluble in water, so it must be mixed with Polythylene Glycol?
True
38
True or False: Lorazepam has a slower onset than Diazepam AND Midazolam?
True
39
Lorazepam: Onset, Peak, E 1/2 Time *How is it metabolized, chemical process?
Onset - 30 minutes Peak - 20-30 minutes E 1/2 Time - 14 hours [glucuronidation]
40
Lorazepam Single Dosing:
1-4 mg IV
41
True or False: Lorazepam has no active metabolites
True
42
What is Flumazenil derived from?
1,4 imidazobenzodiazepine
43
What type of antagonist is Flumazenil? *high or low affinity
Competitive Antagonist; high affinity for BZD receptor
44
True or False: Flumazenil has no active metabolites?
True
45
When is Flumazenil CI?
If pt takes antiseizure meds
46
Flumazenil Dosing: *Repeat dose? *Max dose?
0.2 mg IV Repeat 0.1 mg Q1 min to 1 mg TOTAL
47
Flumazenil Reversal Dosing: *Reverse Sedation *Abolish Therapeutic Dose
*0.3 - 0.6 mg to reverse sedation *0.5 mg - 1.0 mg to abolish therapeutic dose
48
Flumazenil Continuous Infusion Dosing:
0.1-0.4 mg/hr
49
Flumazenil Side Effects:
NONE; just CI in antileptic drugs