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Daddy Pharm > IV anesthetics > Flashcards

IV anesthetics Flashcards

1
Q

T/F
90% of anesthesia is done with propofol

A

False
90% of anesthesia can be done with propofol

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2
Q

emulsion

A

mix of water and oil into continuous form (ie: mayo)
add emulsifying agent (lipid sol end & w. sol end)

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3
Q

Prop emulsion vehicle

A

soybean oil and egg lecithin

used b/c prop isn’t very water soluble

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4
Q

egg lecithin is also known as

A

(an emulsifier)
phosphatidyl choline
serine

naturally occurring in cell membrane

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5
Q

Prop
chemical name & structure

A

2,6-diisopropylphenol
(know how to draw it)

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6
Q

Propofol
class
MoA

A

Unique class of anesthetics

interacts w/ GABA A receptor
decreases GABA dissociation

~ selective with few perceivable effects at other receptors

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7
Q

EDTA

A

disodium edenate
preservative in Diprivan (brand)

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8
Q

Generic prop should not be used in pts with…

A

sulfite allergies
generic contains sodium metabisulfite

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9
Q

Your pt is allergic to wine. Which should you administer?
Diprivan
Generic propofol

A

Diprivan

generic contains sodium metabisulfite
(wines also have sulfites)

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10
Q

Egg lecithin is found in

A

the fatty part of the yolk

not a protein (which pts with egg allergies are most likely allergic to)

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11
Q

Prop induces how quickly?

A

15-30 secs
not as fast as thiopental

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12
Q

How is prop taken up by cells?

A

(very lipid soluble; put into an emulsion)
remains as micelle in BS
outer layer begins brkdwn
oil droplets taken up via endocytosis or absorb across membrane

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13
Q

T/F
Push propofol fast

A

False
painful on injxn

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14
Q

T/F
Hand veins are ideal for propofol administration

A

False
smaller veins a/w more pain on injxn

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15
Q

Mixing propofol w/ liodcaine

A

not recommended
1) lido cant act fast enough
2) breaks emulsion –> oil droplet –> PE

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16
Q

Awakening time faster than with other IV induction agents

A

prop

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17
Q

Less occurrence of post-op hang-over, reports of elevated post-op mood

A

prop

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18
Q

Prop and BZDs have ____ properties

A

anticonvulsant

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19
Q

Prop metabolism
_____ loses most of the compounds activity.
_____ removes it from the body

A

hydroxylation (now 1/3 as active)

glucuronide/sulfate conjugation

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20
Q

Prop
termination of actions d/t…

A

redistribution to fatty tissues and metabolism

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21
Q

Prop metabolism

A

Hepatic and extrahepatic P-450 oxidative metabolism

secondary: phase II glucuronide & sulfate conjugation

High lung uptake but released ~unchanged

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22
Q

Prop metabolism
first [O] rxn

A

form 4 hydroxy diisopropyl phenol (hydroxylate 4th C on ring; “ring hydroxylation”)

becomes point of attachment for glucuronide

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23
Q

Lung metab of propofol

A

not a primary method of metab
but
becomes important for uptake of IAs

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24
Q

Prop
DoE

A

5-10 minutes

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25
Q

Prop
HL

A

2-3 hours

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26
Q

Prop
OB

A

crosses placenta
but
rapidly metabolized by fetus

Pregnancy Category B – no proof of direct risk, however only recommended if benefits outweigh risk

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27
Q

T/F
Liver/renal Dz significantly affects prop elimination

A

False
d/t extra hepatic metab (hydroxylation by tissues outside the liver)

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28
Q

T/F
Prop & BARBs increase pain sensitivity

A

False
prop does not
BARBs do

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29
Q

Prop effects on BP

A

decreased d/t ↓CO & vascular resistance

decreases more than Thiopental

inhibits SNS vasoconstriction

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30
Q

Prop
Increased risk of ___ death, due to ….

A

brady♡-related
inhibition of cardiac sarcolemmal calcium release (blocks muscle activity)

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31
Q

T/F
Skeletal muscle inhibition is seen with Prop.

A

True
inhibition of cardiac sarcolemmal calcium release (blocks muscle activity)

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32
Q

Opioids increase ____ respiration & inhibits the ability to …

A

Cheyne stokes (deep breathing followed by shallow breathing)

sense CO2

caution when using prop with opioids

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33
Q

Prop resp fx

A

Depresses ventilation
apnea in ~30% of patients.

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34
Q

Which accumulates in fat more?
Prop
BARBs

A

BARBs

(they both accumulate in fat but prop has a shorter HL; metabolized out of fat faster)

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35
Q

Prop
when continuously administered for more than 24 hours

A

lactic acidosis
d/t high triglyceride levels

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36
Q

Why does prop cause high TGC?

A

lipid emulsion vehicle

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37
Q

Prop
SEs

A

bradycardia
pain (limited to injxn)
hypertriglyceridemia (lipid emulsion vehicle)
allergic reactions
lactic acidosis (long term infusion)

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38
Q

Fospropofol (Lusedra)

A

propofol prodrug
FDA approve 2008

cleaved to propofol on administration by endothelial alkaline phosphatases

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39
Q

Fospropofol (Lusedra)
current status

A

Dc’d bc not making enough $, but still FDA approved

Could go back into production if shortage of prop

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40
Q

Fospropofol (Lusedra)
pros and cons

A

water soluble (~no pain on injection)

more expensive
half-life (to Propofol) = 8 min (slower onset)
other metabolite = formaldehyde (toxicity in large doses)

41
Q

Propoven

A

different vehicle formulation
more lipids
no preservative
short vial life

42
Q

Propofol Pumps

A

Mechanical syringe presser
Motor pushes on end of plunger
Adjust speed to control rate of infusion

Use with BIS
hold a certain rate of infusion/anesthetic depth

Controversy: Japan company says pump can replace anesthesiologist and use general nursing staff (US protests prevented entry into practice)

43
Q

BIS monitor
___% of normal brain wave activity is considered anesthetized

A

40

44
Q

Etomidate (Amidate)
Structure

A

unlike any other anesthetics
(he did not say to memorize it)

45
Q

propylene glycol toxicity

A

relatively low
avoid very large doses

46
Q

Why makes etomidates HL so short?

A

1) rapid lipid redistribution
2) Metabolized rapidly (ester) hydrolysis of side chain ester group by plasma esterases and hepatic P-450 system

47
Q

Etomidate
MoA

A

GABA-activity enhancement like BARBs and BZDs

GABA A site but unclear location

48
Q

Etomidate is more selective for ___ receptors than the barbiturates

A

GABA A

49
Q

weak base, that’s 99% unionized at physiological pH

A

etomidate

50
Q

Etomidate
protein binding

A

75%

51
Q

Etomidate
Vd

A

large (~300 L) (tissue distribution)

52
Q

Etomidate
time until peak brain concentration

A

w/in 1 min

53
Q

Etomidate
emergence time

A

5-10 mins

54
Q

Etomidate
elim HL

A

2-5 H

55
Q

T/F
Etomidate does not cause any resp depression

A

False
Occasional apnea on rapid administration

Less ventilatory depression than with barbiturates or propofol

56
Q

Etomidate
incidence of myoclonus on rapid IV induction

A

> 80%

57
Q

Etomidate depresses….

A

Depresses steroid (cortisol) synthesis in adrenals

58
Q

T/F
A single dose of etomidate can increase risk of mortality.

A

True

59
Q

Depressed steroid (cortisol) synthesis in adrenals can cause…

A

Increased risk in sepsis and hemorrhage

60
Q

Dexmedetomidine (Precedex)

A

alpha-2 agonist
shuts off norepi release

61
Q

Alpha 2 receptors in brain are mostly

A

pre-synaptic inhibitory
on adrenergic neurons

62
Q

advantage of PREsynaptic inhibition

A

reduces risk of overstimulation
“fine-tuning”

63
Q

Goal when developing Precedex

A

mimic the CNS depressant effects of Clonidine but with better distribution to the brain

64
Q

Dexmedetomidine (Precedex)
uses

A

control of stress, anxiety and pain

used alone: sedates + can arouse to communicate

65
Q

T/F
Placebo can cause sedation

A

True

66
Q

T/F
Adjust Precedex dosing based on age.

A

False
hepatic disease

Pharmacokinetics unaltered by age

67
Q

Precedex
Vd
HL
protein binding

A

Vd ~ 118 liters
t1/2 ~ 2 hrs
~95% protein bound

68
Q

Precedex
Metabolism

A

mainly via glucuronidation (34%) and P-450 hydroxylation

69
Q

Why do we usually give Precedex as a drip?

A

short half-life (~ 2 hrs)

70
Q

T/F
Precedex is lipid insoluble & doesn’t cross BBB

A

False
some lipid solubility; gets into brain

71
Q

Versed
indxn time
DoE

A

~60 secs
~15 mins

72
Q

Versed + opioids

A

for longer durations
greater pain relief than midaz alone

73
Q

T/F
BZDs tend to be highly protein bound
True

A

True
“Versed is 95% plasma protein bound (similar to other benzodiazepines)”

74
Q

T/F
Versed has minimal CV fx

A

True

75
Q

Remimazolam (Byfavo)

A

midazolam analog with an ester linkage (rapid metab)

76
Q

Remimazolam FDA approval

A

2020

77
Q

Remimazolam (Byfavo)
Primary use

A

induction
conscious/ procedural sedation (< 30 min )

78
Q

Remimazolam
SEs

A

hypo/hyperTN
hypoxia (due to hypoTN)

79
Q

Remimazolam vs Versed
duration

A

~ ¼ the duration of an equivalent dose of midazolam

80
Q

T/F
Ketamine can be used IV only

A

False
IV and IM

81
Q

T/F
Ketamine has amnesic effects

A

True
Good analgesic and amnesic

82
Q

Ketamine
action at opioid receptors

A

Blocks Mu
agonist @ Kappa

83
Q

Ketamine
psych instability & hallucinations

A

d/t kappa antagonism/stimulation

84
Q

Ketamine
IV duration

A

15 mins

85
Q

catalepsy (dissociative anesthesia)

A

(Ketamine)
eyes wide open, look awake but don’t respond

blockade of specific neural tracts (block consciousness) + stimulate RAS

86
Q

Ketamine
solubility and protein binding

A

Highly lipid soluble but minimal protein binding

Ketamine:
fat and free

87
Q

Recovery phase characterized by CNS stimulation

A

Ketamine

emerge in quiet & dim (avoid seizures)

88
Q

Adjust Ketamine dosing in the presence of…

A

liver Dz

89
Q

Ketamine MoA

A

Blocks:
glutamate excitatory NMDA receptors (CNS) neuromuscular nACh receptors
Mu receptors

agonism:
Kappa receptors

90
Q

Ketamine
metab

A

N-demethylated (P450) => Norketamine (25% active)

hydroxylation (P450) => hydroxynorketamine (inactive)

Glucuronated & excreted in urine.

90
Q

T/F
Glucuronidation of ketamine inactivates the compound

A

False
hydroxylation (P450) => hydroxynorketamine (inactive)

glucuronidation allows excretion

91
Q

T/F
A pt’s tonic-clonic movements under ketamine can help estimate the depth of anesthesia.

A

False

92
Q

Ketamine should be given slowly bc

A

limit respiratory depression
and
strong vasopressor effects (Possibly life threatening)

93
Q

Ketamine
emergence reaction occurence

A

over 10%

94
Q

Ketamine hallucinations

A

can be dream-like or delirium
possible long term mental health effect
less often in old ppl

95
Q

Ketamine can be given with ___ to reduce the risk of seziures

A

diazepam

96
Q

PF0713

A

propofol analog
less injxn pain
slower onset and longer duration

Benefits questionable – possibly better for maintenance

97
Q

Carboetomidate

A

etomidate analog
“no” adrenal suppression
slower onset

Daddy Pharm (13 decks)

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