Exam 1 - Benzos Flashcards

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
Q

Versed Maintenance Dosing:

26
Q

Versed Postoperative Sedation Dosing:
*Significance of 2-3 Gtt maintenance

A

Dose: 1-7 mg/hr IV
*T-Cell Suppression

27
Q

Is Versed more Water or Lipid Soluble?

A

Water Soluble

28
Q

Is Diazepam more Water or Lipid Soluble?

A

Highly Lipid Soluble

29
Q

True or False: Diazepam is insoluble in water, so it must be mixed with Propylene Glycol?

30
Q

Diazepam: Onset, Peak, E 1/2 time

A

onset: 1-5 min
Peak: Peds - 15-30 min; Adults - 1 Hr
E 1/2 Time: 20-40 hours

31
Q

Diazepam Metabolism:
*Active Metabolites

A

CYP3A
*Desmethyldiazepam and Oxazepam

32
Q

Diazepam CNS Effects: CMRO2 and CBF
*Anticonvulsant Dose
*Isoelectric EEG

A

Decreased CMRO2 and CBF
*Anticonvulsant - 0.1 mg/kg IV
*CAN PRODUCE ISOELECTRIC EEG

33
Q

Diazepam Respiratory Effects:
*Ventilation
*How to reverse Respiratory Depression

A

Minimal effect on ventilation
*Surgical stimulation

34
Q

Diazepam CV Effects:
*BP, CO, SVR
*Change in BP is due to….

A

Minimal decreases in BP, CO, SVR
*BP changes due to synergistic effect with opiates

35
Q

Diazepam Neuromuscular Effects:
*Skeletal muscle tone
*Tolerance?

A

Skeletal muscle tone decreased and can develop a tolerance

36
Q

Valium Induction Dosing:
*Elderly, Liver, Opiates?

A

0.5-1.0 mg/kg IV
*Decreased by 25-50%

37
Q

True or False: Lorazepam is insoluble in water, so it must be mixed with Polythylene Glycol?

38
Q

True or False: Lorazepam has a slower onset than Diazepam AND Midazolam?

39
Q

Lorazepam: Onset, Peak, E 1/2 Time
*How is it metabolized, chemical process?

A

Onset - 30 minutes
Peak - 20-30 minutes
E 1/2 Time - 14 hours [glucuronidation]

40
Q

Lorazepam Single Dosing:

41
Q

True or False: Lorazepam has no active metabolites

42
Q

What is Flumazenil derived from?

A

1,4 imidazobenzodiazepine

43
Q

What type of antagonist is Flumazenil?
*high or low affinity

A

Competitive Antagonist; high affinity for BZD receptor

44
Q

True or False: Flumazenil has no active metabolites?

45
Q

When is Flumazenil CI?

A

If pt takes antiseizure meds

46
Q

Flumazenil Dosing:
*Repeat dose?
*Max dose?

A

0.2 mg IV
Repeat 0.1 mg Q1 min to 1 mg TOTAL

47
Q

Flumazenil Reversal Dosing:
*Reverse Sedation
*Abolish Therapeutic Dose

A

*0.3 - 0.6 mg to reverse sedation
*0.5 mg - 1.0 mg to abolish therapeutic dose

48
Q

Flumazenil Continuous Infusion Dosing:

A

0.1-0.4 mg/hr

49
Q

Flumazenil Side Effects:

A

NONE; just CI in antileptic drugs