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Pharm 2 > Sedative and hypnotics > Flashcards

Sedative and hypnotics Flashcards

1
Q

sedative

A

drug that induces calm of sleep

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2
Q

hypnotics

A

a drug that induces hypnosis or sleep

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3
Q

sleep shares what similarities with anesthesia

A

Inhibits thalmic and mid-brain RAS
Reversibly inhibit CNS

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4
Q

Consciousness/awareness in the OR in how many people (studies)?
What type of cases?
When else might it happen?

A

1-2/1000 in a european study
1/10,000 in another study
- typically happens during sedation cases NOT GENERAL ANESTHESIA
- During emergence

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5
Q

How many levels are there to unconsciousness according to freud?

A

3 concious mind, preconcious, unconscious

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6
Q

When did we discover EEG could measure effects CBF and CMRO2?

A

1937

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7
Q

When was BIS developed?

A

1996

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8
Q

What is BIS?
Lower BIS number correlates how to movement?

A

Bispectral analysis
Lower BIS=Less movement
HIgher BIS = More movement

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8
Q

WHAT ARE the 5 pharmacologic effects of Benzodiazepines?

A
  1. Anxiolytics
  2. Sedation
  3. Anterograde amnesia
  4. Anticonvulsant amnesia
    5.Spinal-Cord mediated skeletal muscle relaxation
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9
Q

What effect of benzos lasts longer than sedation that we must be mindful of?

A

Anterograde amnesia

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10
Q

In 1952 what did we discover that led us to using EEG to monitor depth of anesthesia?

A

we realize depth of anesthesia and and the amount of ether gave correlated.

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11
Q

What effect does using a high dose narcotic technique have on BIS monitoring?
What about hypnotic drugs?

A

There is less correlation between BIS and movement with narcotics.
Hypnotics have a high correlation between BIS and movement

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12
Q

BIS < 58 correlated with?

A

Loss of conciousness

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13
Q

BIS < 65 had what correlation?

A

Had less than 5% chance of return to conciousness within 50 seconds

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14
Q

What is SQI?

A

Signal Quality Index, tells us whether or not we have a good signal or if we have a lot of artifact.

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15
Q

what is EMG?

A

Electormyography and it tells us information about muscle activity and if the patient can move.

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16
Q

What is EEG?

A

Electroencephalogram, this tells information about brainwave activity.

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17
Q

What is SR?
What do we want this number to be?

A

Suppression Ratio, this tells us how many seconds in the last minute that the EEG has been flat.
We want this number to be zero.

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18
Q

What is typical number we want our BIS to be during general anesthesia cases?

A

40-60

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19
Q

What drugs may decrease your BIS number?

A
  • volatlies
  • hypnotics
  • NMBD
  • opioids
20
Q

What drugs may increase your BIS number? why?

A

Ketamine and Epinephrine
* Stimulates your sympathetic system, this would be a falsely high reading

21
Q

What drug may artificially lower your BIS score due to lower CMRO2 and CBF?

A

Betablockers, decrease HR = Decrease CO = decrease CBF= decrease CMRO2

22
Q

What are 4 benefits of benzos over barbs?
What do we use benzos for in anesthesia?

A

Less tolerance

Less potential for abuse

Fewer and less serious side effects

Do not induce hepatic microsomal enzymes

***Have replaced barbiturates for preop sedation

23
Q

What is the antagonist for benzodiazpines?

A

Romazicon (flumazenil)

24
Q

Which benzo is the most common preop sedative?

A

Versed (midazolam)

25
Q

Which has a longer 1/2 time, midazolam (versed) or Lorazepam (ativan)?

A

Lorazepam (Ativan)

26
Q

What is the MOA of benzodiazepines?

A

GABA mediated, So they bind to a receptor site specific to benzos and they increase the affinity of the GABA receptor. Once the GABA receptor is stimulated the the Cl- channel opens and causes hyperpolarization of the postynaptic membrane which makes it more difficult to depolarize again

27
Q

Describe the different receptor sites of the GABA A receptor.

A
28
Q

What kind of effects do the alpha-1 stimulatory drugs have?
Where do they have their action?

A
  • Sedative, amestic, anticonvulsant
  • Cerebral cortex, cerebellar cortex and thalamus
29
Q

What kind of effects do alpha-2 receptors have? where do they have their action?

A
  • anxiolytic and skeletal muscle relaxation
  • hippocampus and amygdala
30
Q

What other drugs bind to GABA A receptors?
Why does this matter if you’re giving benzos?

A
  • Barbituates
  • Etomidate
  • propofol
  • alcohol
    They will have synergistic effects and increase the likelyhood of OD or may have a cross-tolerance
31
Q

What 4 things can cause differences in onset and duration between drugs of the same class?

A

Potency (receptor binding affinity)
lipid solubility (crossing the BBB)
Redistribution (to peripheral tissues)
Pharmacokinetics (ADME)

32
Q

What effect do benzos have on platelets?

A

they can inhibit platelet aggregating factor, inability to have conformational change so they can aggregate

33
Q

What is an important feature of Versed’s chemical structure?

A

imidazole ring, this stabilizes the structure and allows for rapid metabolism

34
Q

What is the main indication of midazolam for anesthesia?

A

Pre op med and conscious sedation

35
Q

How much more potent is midazolam (versed) than diazepam (valium)?

A

2-3x more potent

36
Q

Is versed lipid or water soluble?
What is the parenteral solutions pH?

A

water soluble.
3.5

37
Q

How does the imidazole ring start out at 3.5 pH?

A

the imidazole ring is open, making versed water soluble (protonated)

38
Q

What happens to the imidazole ring when you inject versed

A

It closes at a pH of 4.0, which makes it lipid soluble and unprotonated

39
Q

What is the benefit of versed being water soluble and not needing propylene gylcol to stabilize it?

A

it doesnt burn upon injection

40
Q

Versed
onset?
peak?
Protein binding?
Duration?
1/2 time? (elderly?)
Vd? (elderly / obese)
Metabolism?
active Metabolites?
What drugs we commonly use that inhibit the CYP450 enzyme activity?
Clearance in comparison to ativan? and valium?

A
  • 1-2 mintutes onset
  • 5 minutes peak
  • highly protein bound (96-98%)
  • Short duration d/t lipid solubility
  • 2 hours, doubles in elderly
  • 1-1.5 L/kg (LARGE)
  • Vd increases in the elderly and obese because they both have more fat RELATIVE to the normal person.
  • elderly people have less muscle mass and more fat mass.
  • CYP3A4
  • Active metabolites- 1-hydroxymidazolam, has half the activity of parent molecule
  • DRUGS: cimetidine, erythromycin, CCB, antifungals, fentanyl
  • Clearance of versed is 5x faster than ativan and 10x faster than valium
41
Q

VERSED
CNS?

A

CNS- Dose related decrease of CMRO2 and CBF; Potent Anticonvulsant even in status; perserves vasomotor response; doesn’t change ICP; cannot produce isoelectric EEG

42
Q

VERSED
Pulm?

A

DOSE DEPENDENT decrease in hypoxic drive, worse in COPD. Can cause transient apnea (especially if if give with opioid) Supresses swallowing & upper airway activity (coughing) –> risk of ASPIRATION

43
Q

VERSED
CV?

A

Increases HR; decreases BP. CO is maintained. Decreases SVR

44
Q

VERSED
Dosing for sedation?
Peds? Adult? Elderly?

A

Peds PO: 0.25 - 0.5 mg/kg (syrup so peak effect is 20-30 min)
Adults IV: 1 - 5 mg; Peak 5 minutes; elderly require decreased dose d/t > CNS activity

45
Q

VERSED
Induction?
What facilitates induction with versed?

A

IV : 0.1 - 0.2 mg/kg over 30 - 60 secs; give with Fentanyl 50-100 mcg 1 - 3 mins prior
Facilitated by preceding dose of opioid within 1-3 minutes, Fentanyl 50-100 mcg

46
Q

VERSED
Maitneance?
Supplemental with?
Rarely associated with?

A

Uncommon ;
Can be used to supplement opioids, propofol, volatiles;
Rarely associated w/ N/V or emergence excitement

47
Q

VERSED
Post op sedation?
consideration with IV drip length of time and what happens?

A

IV gtt: 1 - 7 mg/hr
Prolonged gtt > 3 days: T-cell Suppression

Pharm 2 (4 decks)

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