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Pharm Spring 2024 > Sedatives/Hypnotics > Flashcards

Sedatives/Hypnotics Flashcards

1
Q

Define sedatives

A

A drug that induces calm or sleep

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2
Q

Define hynotics

A

A drug that induces hypnosis or sleep

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3
Q

What does having a high CBF/CMRO2 mean?

A

Awake/Active

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4
Q

What does having a low CBF/CRMO2 mean?

A

Less awake/active

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5
Q

On the EEG wires define what the Z leads are, where the odd #’s go, where the even numbers go, and what T, F, P, & O mean.

A

Z leads - the reference point
Odd numbers - left side
Even numbers - right side
T- Temporal
F- Frontal
P - Parietal
O- Occipital

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6
Q

What is the BIS machine? When did it come out?

A

A machine that took all the info & leads from the EEG wires & combined them into 1 waveform.
Developed in 1996

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7
Q

Is a patient with a BIS < 58 consious?

A

No; also no change in HR, BP.

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8
Q

If the BIS <65 what happens? At what percent does this happen?

A

The patient has less than a 5% chance of returning to consciousness within 50 seconds. Have a least a minute to get the patient deeper before they wake up and move.

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9
Q

What is SQI?

A

Signal Quality Index. How much or little interference.

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10
Q

Define EMG. Do we want to see this?

A

Muscle tension detection. No want to see zero EMG.

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11
Q

If things are going well what should we see for the EEG on the BIS?

A

Should be fairly flat

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12
Q

Define SR.

A

Suppression Ratio - tells us how many times in the last 20-30 seconds the BIS has been Zero. Tells us how many times the EEG was flat. Don’t want to see this climb.

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13
Q

What do you want to see for the SR? How does this differ in brain-dead patients?

A

Flat essentially.
Will have a high suppression ratio - because there is zero activity.

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14
Q

What range on the BIS is the patient awake?

A

98-100

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15
Q

What number on the BIS correlates with patient having eyes closed/quiet/dreaming?

A

85-90

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16
Q

What number on the BIS appears with GA?

A

40-60

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17
Q

If the patient has a BIS > 60 what are they at risk for?

A

MOVING

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18
Q

At what range on the BIS can the patient self extubate?

A

70-80

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19
Q

What does a BIS reading of 40 indicate?

A

Too deep, wasting our drugs, gave too much

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20
Q

What are some benefits of using benzos?

A

Sedation
Anxiolytics
Anticonvulsants

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21
Q

What kind of amnesia do benzo’s cause? (Think versed)

A

Anterograde

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22
Q

Why are benzos better than barbs?

A

Less tolerance
Less addiction
Less potential for abuse
Few and less serious side effects
Do not induce hepatic microsomal enzymes

23
Q

What is the benzo of choice for the perioperative period?

A

Midazolam (Versed)

24
Q

What is the benzo of choice for the post-op period?

A

Diazepam or Lorazepam

25
Q

What drug is replacing Lorazepam during the post-op period? What are its side effects?

A

Dexmedetomidine. Causes bradycardia

26
Q

What is the primary MOA of benzos?

A

Facilitates the action of GABA at the GABAa chloride ionophore. They are an allosteric activator. They bind to the benzo receptors, which help GABA bind to its receptor better.

27
Q

What does the alpha 1 do? Is it the most abundant type? What parts of the brain

A

Sedative, amnestic, anticonvulsant.
Yes
Cerebral cortex, cerebellar cortex, thalamus

28
Q

What does the alpha 2 do? Its location in the brain?

A

Anxiolytic
Skeletal muscle
Hippocampus and amygdala

29
Q

Where are GABAa receptors primarily?

A

CNS

30
Q
A
31
Q

What other medications bind to GABAa?

A

Barbiturates
Etomidate
Propofol
Alcohol

32
Q

What diseases/issues cause decreased albumin levels? What effect does this have on benzos?

A

Cirrhosis, burns, elderly, malnutrition
Increases the free drug; more crosses the BBB & causes increased effects.

33
Q

Which drug will cause an isoelectric state on the EEG? Which drug will not cause an isoelectric state on the EEG?

A

Diazepam
Versed

34
Q

At what pH is versed’s ring open and it is water soluble and in the protonated form?

A

<3.5

35
Q

At what pH does the versed ring close and it becomes lipid soluble?

A

> 4.0

36
Q

Define versed’s onset, peak effect, E 1/2 time, & Vd

A

Onset 1-2 mins
Peak effect - 5 mins
E 1/2 time - 2 hrs
Vd - 1 to 1.5 L/kg

37
Q

How is versed metabolized?

A

CYP3A4
Active metabolites conjugated and cleared by kidneys

38
Q

Name the active metabolite of versed mentioned in class. How potent is it?

A

1-hydroxymidazolam. 1/2 the activity of the versed

39
Q

What drugs can cause inhibition of the CYP450s?

A

Cemetidine (Tagament -PPI)
Erythromycin
CCBs
Antifungals
Fentanyl

40
Q

How much faster is versed cleared compared to lorazepam? Diazepam?

A

5x faster than lorazepam
10x faster than diazepam

41
Q

What benzo do you use for induction if the patient has a neuro pathology?

A

versed

42
Q

How is valium prepared? Why is it prepared this way?

A

Dissolved in organic solvents have to use propylene glycol (which hurts during injection). Valium is insoluble in H2O.

43
Q

Describe the pharmacokinetics of valium

A

Onset 1-5 mins
E 1/2 time 20-40 mins
Similar Vd to versed
Dissociates from GABAa faster than ativan
Uses the CYP3A pathway. Has 2 active metabolites

44
Q

Name the 2 active metabolites of diazepam

A

Desmethyldiazepam - 48 to 96hrs - nearly as potent as diazepam
Oxazepam

45
Q

Diazepam is a decent choice for what in patients that have this condition?

A

Anxiolysis/muscle relaxation with COPD patients

46
Q
A
47
Q

How much do you decrease diazepam dose in elderly, liver disease, & presence of opioids? Why do you reduce the dose?

A

25-50%
Because of active metabolites

48
Q

What drug is great for post-op sedation?

A

Ativan

49
Q

What drug’s metabolite does ativan resemble?

A

Oxazepam a metabolite of diazepam

50
Q

What drug is a more potent sedative than midazolam & diazepam?

A

ativan

51
Q

Is ativan soluble in water? What solvent does it require?

A

No, needs polyethylene glycol. That’s why it burns

52
Q

What benzo is the slowest to end the CNS

A

ativan

53
Q

Describe peak effect & at what dose, E 1/2 time, & clearance of ativan

A

Peak effect is 20-30mins with IV dose of 1-4mg
E 1/2 time is 14 hours
Not entirely dependent on hepatic enzymes

54
Q

What is the antidote for benzos? How is it dosed? How long until you see reversal effects? How long does it last?

A

Flumazenil (Romazicon)
0.2mg IV & titrate to consciousness
Repeat 0.1mg every 1 minute to 1mg total
Reversal within 2 mins
Duration is 30-60 mins

Pharm Spring 2024 (7 decks)

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