Sedatives/Hypnotics

Question 1

Define sedatives

Answer 1

A drug that induces calm or sleep

Question 2

Define hynotics

Answer 2

A drug that induces hypnosis or sleep

Question 3

What does having a high CBF/CMRO2 mean?

Answer 3

Awake/Active

Question 4

What does having a low CBF/CRMO2 mean?

Answer 4

Less awake/active

Question 5

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.

Answer 5

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

Question 6

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

Answer 6

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

Question 7

Is a patient with a BIS < 58 consious?

Answer 7

No; also no change in HR, BP.

Question 8

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

Answer 8

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.

Question 9

What is SQI?

Answer 9

Signal Quality Index. How much or little interference.

Question 10

Define EMG. Do we want to see this?

Answer 10

Muscle tension detection. No want to see zero EMG.

Question 11

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

Answer 11

Should be fairly flat

Question 12

Define SR.

Answer 12

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.

Question 13

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

Answer 13

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

Question 14

What range on the BIS is the patient awake?

Answer 14

98-100

Question 15

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

Answer 15

85-90

Question 16

What number on the BIS appears with GA?

Answer 16

40-60

Question 17

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

Answer 17

MOVING

Question 18

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

Answer 18

70-80

Question 19

What does a BIS reading of 40 indicate?

Answer 19

Too deep, wasting our drugs, gave too much

Question 20

What are some benefits of using benzos?

Answer 20

Sedation
Anxiolytics
Anticonvulsants

Question 21

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

Answer 21

Anterograde

Question 22

Why are benzos better than barbs?

Answer 22

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

Question 23

What is the benzo of choice for the perioperative period?

Answer 23

Midazolam (Versed)

Question 24

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

Answer 24

Diazepam or Lorazepam

Question 25

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

Answer 25

Dexmedetomidine. Causes bradycardia

Question 26

What is the primary MOA of benzos?

Answer 26

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.

Question 27

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

Answer 27

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

Question 28

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

Answer 28

Anxiolytic Skeletal muscle Hippocampus and amygdala

Question 29

Where are GABAa receptors primarily?

Answer 29

CNS

Question 31

What other medications bind to GABAa?

Answer 31

Barbiturates Etomidate Propofol Alcohol

Question 32

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

Answer 32

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

Question 33

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

Answer 33

Diazepam Versed

Question 34

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

Answer 34

<3.5

Question 35

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

Answer 35

>4.0

Question 36

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

Answer 36

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

Question 37

How is versed metabolized?

Answer 37

CYP3A4 Active metabolites conjugated and cleared by kidneys

Question 38

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

Answer 38

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

Question 39

What drugs can cause inhibition of the CYP450s?

Answer 39

Cemetidine (Tagament -PPI) Erythromycin CCBs Antifungals Fentanyl

Question 40

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

Answer 40

5x faster than lorazepam 10x faster than diazepam

Question 41

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

Answer 41

versed

Question 42

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

Answer 42

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

Question 43

Describe the pharmacokinetics of valium

Answer 43

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

Question 44

Name the 2 active metabolites of diazepam

Answer 44

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

Question 45

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

Answer 45

Anxiolysis/muscle relaxation with COPD patients

Question 47

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

Answer 47

25-50% Because of active metabolites

Question 48

What drug is great for post-op sedation?

Answer 48

Ativan

Question 49

What drug's metabolite does ativan resemble?

Answer 49

Oxazepam a metabolite of diazepam

Question 50

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

Answer 50

ativan

Question 51

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

Answer 51

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

Question 52

What benzo is the slowest to end the CNS

Answer 52

ativan

Question 53

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

Answer 53

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

Question 54

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

Answer 54

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