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Pharmacology > Propofol, Etomidate > Flashcards

Propofol, Etomidate Flashcards

1
Q

propofol chemical name

A

2, 6 di-iso-propophenol

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2
Q

propofol is mixed with:

A

1.2% egg
10% soybean
2.25% glycerol base

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3
Q

propofol draw up safety

A

supports bacterial growth, never use same bottle

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4
Q

propofol extended infusion efect

A

increased glycerides

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5
Q

propofol allergies

A

egg yolk allergies, anaphylactic

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6
Q

2 ways propofol is supplied

A

Diprivan EDTA - ok

Propofol Sodium Metabisulfite - bronchospasms

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7
Q

propofol mechanism of action

A

GABAa, Glycine
decreases rate of dissociation of GABA from GABAa
no spinal cord depression

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8
Q

propofol Vd, clearance, model of distribution, T1/2

A

3.5-4.5 L/Kg
clearance exceeds hepatic blood flow
2-3 compartment model
T1/2 - 0.5-1.5 hrs

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9
Q

propofol: what affects pharmacokinetics

A

weight, co-existing disease, age, co-administration with other drugs

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10
Q

propofol CNS effects specifics

A

chloride channel activation of B subunit of GABA receptor, NMDA inhibition

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11
Q

propofol CNS effects

A 
rapid onset, one arm-brain circulation
decreases CMRO2, CBF, ICP, CPP, cerebral protective
EEG burst suppression
age effects ED95 - highest in toddlers, decreases with age
hiccups, muscle twitching
hallucinations, opisthotonos
decreased IOP
antioxidant effects
myoclonus
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12
Q

propofol respiratory effects

A 
apnea following induction
decreases TV, RR
decreased response to CO2 and hypoxia
PaCO2 rises, pH decreases
bronchodilation in COPD
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13
Q

propofol CV effects

A 
25-40% decrease in BP
greater than with STP
dose dependent myocardial depression and vasodilation
similar decrease in SV, CO, SVR
HR UNCHANGED
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14
Q

propofol other effects

A 
does not potentiate muscle relaxants
pain on injection
antiemetic/antipruritic at 10 mg doeses
amnestic at >30 mcg/kg/min
crosses placenta, removed from fetal circulation
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15
Q

propofol doses

A

induction 1-2.5 mg/kg up to 3 mg/kg in toddlers
GA maintenance infusion 100-300 mcg/kg/min
sedation infusion 25-100 mcg/kg/min

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16
Q

propofol metabolism

A

conjugated in liver by CP 450
liver function does not affect rate of metabolism
metabolites mostly inactive
4-hydroxypropofol is 1/3 as potent
CKD doesn’t affect clearance
highly metabolised, less than 3% excreted unchanged

17
Q

etomidate derivative name, parent compound, solvent name, pH

A

carboxylated imidazole derivative
imidazole refers to the parent compound C3H4N2
propylene glycol solvent
pH 6.9 - water soluble in solution
at physiological pH, becomes highly lipid soluble

18
Q

etomidate mechanism of action

A

selective GABAa
binds to specific receptor
increases affinity of GABA to GABAa

19
Q

etomidate onset of action, solubility, Vd, compartment model, T1/2, protein bound %

A 
rapid onset of action
highly lipid soluble
weak base pH 8.2
Vd 2.5-4.5 L/Kg
3 compartment model
T1/2 3-5 hrs
high hepatic extraction ratio - changes in hepatic blood flow will prolong effect
75% protein bound
20
Q

etomidate CNS effects

A 
rapid loss of consciousness
no analgesia
direct cerebral vasoconstriction, decrease CBF, ICP, CMRO2
reduced IOP
increases EEG activity in epileptogenic foci
rare association with Grand Mal siezures
myoclonic movement
anticonvulsant
21
Q

etomidate respiratory effects

A

minimal ventilatory response to CO2 drop
decrease in TV, increase in RR
hiccups, coughing

22
Q

etomidate CV effects

A

minimal effects on CV, b/c no effect on SNS and baroreceptors

23
Q

etomidate endocrine effects

A

dose dependent reversible inhibition of 2 enzymes in biosynthesis of cortisol/aldosterone

24
Q

etomidate 2 enzymes

A

11 betahydroxylase
17 alphahydroxylase
prevents conversion of cholesterol to cortisol
results in adrenocortical suppression for 4-8 hrs
reduces mineralcorticoid and corticosteroid production

25
Q

etomidate and same day surgery

A

not ideal, too much N/V

26
Q

etomidate dosage

A

induction 0.2-0.6 mg/kg (0.3 mg/kg)
maintenance infusion 10 mcg/kg/min w/ N2O and opioids
sedation 5-8 mcg/kg/min for short procedure
rectal 6.5 mg/kg has been used in peds

27
Q

etomidate and N/V

A

high incidence of N/V 30-40%
myoclonic movement 30-60%
enhance NMDR activity

28
Q

etomidate metabolism

A

liver, ester hydrolysis or N dealkylation to carboxylic acid
biotransformation 5x faster than thiopental
85% renal, 13% biliary excretion
2% excreted unchanged

Pharmacology (7 decks)

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