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N926 Pharmacology > Induction agents > Flashcards

Induction agents Flashcards

1
Q

sedative-hypnotics major functions

A
  • sedative
  • hypnotic
  • axiolytic
  • general anesthetic
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2
Q

In a perfect world….

A
  • stable in aqueous solution: water soluble
  • minimal major cardio or resp depression
  • rapid metabolism
  • steep dose respose curve
  • rapdi return to mental baseline
  • rapid and smooth onset
  • Lack of hypersensitivity
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3
Q

What other substance is added to propofol? Their %

A

10% Soybean oil

  1. 25% glycerol
  2. 2% egg lithecin
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4
Q

Three propofol unique properties

A
  • non-chiral
  • pain on injecftion
  • rapid return to consciousness
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5
Q

Two brands of propofo

pH, pK and additives

A
  • Diprivan 7-8.5, 11, EDTA
  • Propofol 4.5-6.4, 11, sodium metadisulfite or benzyl alcohol
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6
Q

Propofol MOA

Effect on spinal

A

selective GABA selective modulator

Spinal motor neuron excitability not altered

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7
Q

Propofol unique metabolism mechanism

A

Clearance exceeds hepatic blood flow:

  • Tissue uptake in lungs
  • extensive hepatic metabolism CYP450
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8
Q

Propofol metabolite

A

4-hydroxypropofol

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9
Q

Propofol context sensitive t1/2

A

<40min

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10
Q

How is propofol affected by hepatic or renal dysfunction?

A

Not influenced.

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11
Q

for propofol, Decreased rate of plasma clearance in pt over what age?

A

60.

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12
Q

What does propofol bind to and their %.

A

Erythrocytes and plasma proteins (50%)

plasma albumin (48%)

Free (2%)

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13
Q

In what population do you see increased free fraction?

A
  • Severe heaptic and renal disease
  • pregnant woman
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14
Q

Is propofol an acid or base?

A

Acid

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15
Q

How is myoclonous induced in propofol?

A

2ndary to disinhibition of subcortical centers

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16
Q

How does propofol cause moderate BP decrease?

A
  • Primary decrease in sympathetic tone and vasodilation (primary)
  • CNS, cardiac and baroreceptor depression
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17
Q

How does propofol affect respiratory depression?

A

Dose dependent with infusions secondary to decreased sensitivity of respiratory center to CO2

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18
Q

Propofol broncho effect?

A

minimal bronchodilation

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19
Q

Propofol induction dose?

A

1.5-2.5mg/kg

  • Decrease dose in elderly
  • Increase dose in pediatrics
  • Effects exaggerated with CV disease
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20
Q

What kind of Monitored Anesthesia Care is porpofol good for?

A

endoscopy

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21
Q

What is the dose of propofol for monitored anesthesia care?

A

25-100 mcg/kg/min

Can be used in conjunction with anxiolytic and opioid

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22
Q

What is the dose of propofol for TIVA

A

100-300 mcg/kg/min

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23
Q

Other applications of propofol and doses

A

animetics 10-15mg IV, followed by 10mcg/kg/min gtt

antipruritic 10mg IV

anticonvulsant 1mg/kg IV

Attenuante bronchoconstriction, through Ca++ homeostasis

analgesic for neuropathic pain

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24
Q

Propofol contraindications

A
  • olderly, cardiac compromised
  • sulfate allergy, more in asthmatic pt
  • lecithin alergy
  • lipid metabolism disorder
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25
Q

PRIS risk factors

A

>4mg/kg/hr, >48hrs

critical illness

high fat-low carb intake

concomitant catecholamine infusion, steroid administration and inborn errors of mitochondrial fatty acid oxidation

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26
Q

PRIS signs and symptoms

A
  • high anion gap (AGMA)
  • fever
  • cardiac failure
  • bradycardia refractory to treatment
  • severe hepatic and renal disturbances
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27
Q

% of academic centers reporting abuse or diversion of propofol

A

18

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28
Q

Is etomidate an acid or base? pH, pK?

A

it is a weak base, 8.1, 4.2

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29
Q

When do you use etomidate?

A

unstable cardiac pt

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30
Q

What structure does etomidate have?

A

carboxylated imidazole

R+ isomer 5x more potent

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31
Q

etomidate MOA

A

selective modulator of GABAa receptors

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32
Q

how much is etomidate bound to lipid?

A

75% boiund to plasma albumin

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33
Q

rank the three induction agents in terms of protein bound

A

propofol (98%)>etomidate(75%)>ketamine (12%)

34
Q

unique metabolism function of etomidate

A

metabolized by hydrolysis, plasma esterase and microsomal enzymes in liver

35
Q

etomidate onset and return to conscious time

A

rapid onset: one arm to brain circulation

return to consciousnewss 5-15 min

36
Q

What kind of movement happens when given etomidate?

% of pt having this problem?

why?

A

myoclonus movement common.

happens in 50% of pt

Secondary to deep cerebral and brainstem.

37
Q

Starting from what dose does etomidate cause changes in HR, stroke volume, or C.O.

And at what dose there is significant change in SBP?

A

0.3mg/kg and 0.45mg/kg

38
Q

Which drugs causes apnea during rapid iv injection?

A

etomidate

39
Q

etomidate induction dose

A

0.2-0.4mg/kg

40
Q

What kind of pt is more prone to myoclonus movement?

A

Young

41
Q

giving etomidate, % of patients that will show myoclonus movement.

A

>50%

42
Q

how to decrease incidence of myoclonus movement?

A

given fentanyl and benzo

43
Q

In etomidate, what causes adrenocortical suppression?

A

11-Betahydraxylase inhibits cholesterol converting to cortisol

44
Q

how long does etomidate adrenocortical suppression last?

A

greater than 8 hrs after induction.

45
Q

GI effect of etomidate.

A

Nausea and vomiting

46
Q

Does etomdiate cause pain on injection?

A

Minimal. Used to, new solvents not anymore

47
Q

Which drugs cause porphyria?

A

Barbs and etomidate, plus, benzos

48
Q

How does EEG look like for pt on ketamine?

A

disassociation between thalamocortical and limbic systems

49
Q

What state do pt get into when given ketamine? How does it look like

A

cataleptic state. eyes remain open with slow nystagmic gaze.

50
Q

How does Ketamine disolve?

A

does not require a lipid “vehicle” for dissolution

51
Q

ketamine acidity, pH, pk

A

it is a base, ph 3.5-5.5, pk, 7.5

52
Q

How is ketamine metabolized?

A

demethylation of ketamine by cyp450.

  • metabolism dependent on hepatic flow
  • norketamine is active metabolite, then broken down to water soluble and inactive metabolites
53
Q

ketamine t1/2

A

2-3 hrs

54
Q

how is ketamine lipidphility?

A

highly lipid soluble, rapid transfer BBB

55
Q

What does NMDA stand for?

A

N-methyl-D-apartate

56
Q

ketamine MOA

A

binds non-comptetively to phencyclidine site on NMDA receptors to block glutamate, resulting in depressive effect on the medial thalmic nuclei.

57
Q

receptors ketamine work on

A

opioid, monoaminergic, muscarinic, voltage gated sodium, L type calcium, and nAchR

58
Q

Other way ketamine have analgesic effect

A

directly inhibition of cytokines

59
Q

which system is activated by ketamine?

A

limbic system

60
Q

Does ketamine have effect on GABA?

A

weak action on GABAa receptors

61
Q

ketamine eye, airway, muscular skeletal effect

A

eyes open, pupils reactive, corneal reflex intact, nystagmus present, lacrimation and blinking continue. IOP increases, do not use in eye procedures.

airway reflex intact, increased salivary secretions,

increased skeletal muscle tone

62
Q

When using ketamine, what other agents should be given as well?

A

some analgesics or benzos, like fentayl to decrease hallucination and decrease ICP

63
Q

What type of pt can benefit from ketamine’s bronchodilation effect?

A

asthmatic

64
Q

What is patient population is ketamine for?

A

hypovolemic trauma

65
Q

ketamine induction doses and response times

How would you describe its response time?

A

1-2.5mg/kg IV (2-3min)

4-8mg/kg IM (<10min)

10mg/kg PO (10-20min)

They take longer, compared to propofol and etomidate, seconds

66
Q

Does ketamine cause pain?

A

no pain on injection

67
Q

ketamine induction on CAD patient?

A

it is complicated.

68
Q

ketamine subanesthetic dose for analgesic effect

A

0.2-0.5mg/kg

69
Q

what receptors sensitizes spinal cord?

A

NMDA receptors

70
Q

Why is ketamine used in OB anesthesia?

A

Does not compromise uterine tone, blood flow or neonatal status.

71
Q

What type of trauma patient is ketamine used for, what procedure?

A

Burn patients, with extensive dressing changes and grafting procedures.

72
Q

What is ketamine dart used for

A

pediatric asthmatic patient.

73
Q

What can ketamine do to chronic pain mgnt?

A

opioid induced hyperalgesia, treatment for CRPS and cancer pain.

74
Q

What effect does ketamine have on sux?

A

inhibit plasma cholinesterase, prolonged apnea

75
Q

what effect does ketamine have on non-depolarizing NMBA?

A

enhancement

76
Q

what medication should be avoided for pt at risk of MI during preop period if ketamine is given?

A

medication that block preconditioning

77
Q

% of pt experience emergence delirium after using ketamine

A

5-30%, partially dose dependent

78
Q

how long does the emergence delirium last after ketamine admin?

A

can occur up to 24 hrs

79
Q

have morbid and vivid color d/t depression of what part of brain?

A

inferior coolliculus and medial geniculate nucleus

80
Q

emergence delirium risk factors

A

>15 yrs old, female, hx personality problem or frequent dreams.

81
Q

which benzo used prior to ketamine decrease emergence delirium better

A

midazolam>diazepam

82
Q

which agent can increase emergence delirium?

A

atropine

N926 Pharmacology (16 decks)

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