Neuromuscular Blocking Agents Flashcards

1
Q

Succ MOA

A

Mimics the action of Ach.
2 molecules of Ach linked by acetate methyl groups.
Partial agonist at nicotinic Ach receptors and attaches to one or both of the alpha subunits
depolarizing the ion channels at the post junctional membrane.
Sustained opening and depolarization prevents propagations of a new action potential.

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2
Q

Succ USE

A

Tracheal intubation

immobility during surgery

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3
Q

Succ Dose IV

A

1 mg/kg

range 0.3-1.1 mg/kg

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4
Q

Succ Dose IM

A

3-4 mg/kg

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5
Q

Succ Onset

A

30-60 seconds

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6
Q

Succ Duration

A

4-6 minutes

very short acting

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7
Q

Succ Peak

A

30-60 seconds

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8
Q

Succ Elimination

A

Excreted in the Urine

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9
Q

Succ metabolism

A

Hydolysis

Plasma Pseudocholinesterases

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10
Q

Succ Adverse reaction

A
Cardiac
Hyperkalemia
Myalgia
Myoglobinuria
IIOP
IICP
Salivation
Histamine Release *rare
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11
Q

Succ Contraindications

A
Hypersensitivity/anaphylaxis 
*peds dt Duchennes 
Open globe
MH
Atypical plasma cholinesterase
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12
Q

succ classification

A

dicholine ester depolarizing neuromuscular blocker

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13
Q

Brand name of Succ

A

Anectine

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14
Q

How is Succ supplied?

A

20 mg/mL
10 mL vial
200 mg total

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15
Q

Brand name of Vecuronium

A

Norcuron

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16
Q

How is vec supplied?

A

1mg/mL

10 mg reconstitute to 1 mg/mL

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17
Q

Mechanism of Action of Vec

A
competitive antagonist with ACh
at the nicotinic cholinergic receptor
post synaptic membrane end plate 
bind to 1 alpha subunit --> NMB
some presynaptic effect
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18
Q

what is Vec used for?

A

Tracheal intubation
Immobility during surgery
Facilitate mechanical
Ventilation

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19
Q

intubating dose of Vec

A

0.08-0.12 mg/kg

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20
Q

maintenance dose of Vec

A

0.01-0.015 mg/kg

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21
Q

dose for shivering with Vec

A

8-12 mg

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22
Q

onset of vec

A

2.5-3 minutes

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23
Q

DOA of vec

A

20-35 minutes
longer with elderly
45-65 minutes

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24
Q

peak of vec

A

3-5 minutes

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25
Q

half life of vec

A

65-75 minutes

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26
Q

elimination of vec

A

biliary: excretion/feces (40-75 %)
renal 25-35 %
redistribution and reversal in Cholinesterase I primary way to stop blockade

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27
Q

metabolism of vec

A

minimal hepatic
spontaneous deacetylation
active metabolite

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28
Q

Adv reactions with Vec

A

RARE- CV- bradycardia with opiods

cv collapse, edema, flushing, hypersensitivity reaction

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29
Q

contraindications with vec

A

Hypersensitivity/anaphylaxis reaction

BURN patients (>30% will be resistant for 5-7 days post insury)

Immobilization

Acute Quadriplegic Myopathy Syndrome in patients taking corticosteriods

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30
Q

brand name of Rocuronium

A

Zemuron

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31
Q

How is Rocuronium supplied?

A

10 mg/mL

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32
Q

classification of Rocuronium

A

intermediate acting
monoquaternary aminosteriod NDMB
derivative of vecuronium
it was designed to speed onset- less potent- more drug given able to occupy more receptors

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33
Q

MOA rocuronium

A
competitive antagonist with ACh
at the nicotinic cholinergic receptor
post synaptic membrane end plate 
bind to 1 alpha subunit --> NMB
some presynaptic effect
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34
Q

use of roc

A

Tracheal intubation
Immobility during surgery
Facilitate mechanical
Ventilation

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35
Q

intubating dose of roc

A
  1. 45-9 mg/kg

0. 6 mg/kg

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36
Q

RSI dose for roc

A

0.6-1.2 mg/kg

1 mg/kg approaches the onset of such 30-60 sec

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37
Q

maintenance dose of rocc

A

0.1-0.2 mg/kg

10-20 minutes per dose of maintenance

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38
Q

defasciculation dose of roc

A

0.03-0.06 mg/kg

give 1.5-3 minutes before succ

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39
Q

onset of roc

A

1-2 minutes for intubating dose

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40
Q

peak of roc

A

4 minutes

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41
Q

half-life of roc

A

60-144 minutes

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42
Q

elimination of roc

A

feces 50%
urine 30%
reversal is primarily from redistribution
gradual metabolism
excrete gradually
Cholinesterase- Inhibitors inhibit acetylcholinesterase enzyme activity, stops Ach-esterase activity, increase Ach, stop block

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43
Q

metabolism of roc

A

Minimal hepatic

5-10% activity of the parents drug

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44
Q

Adverse reactions of Roc

A

Slight vagolytic tendencies- increase HR

HTN/HypoTN

Anaphylactoid rxn

RHF worsensed

Vessel irritant

Rare- ECG changes, anaphylactoid, anaphylaxis, arrhythmis, bronchospasm, edema at lite, hiccupts, pruritis, nausea, PVR increased, rash, rhonchi, shock, tackycardia, vomiting, wheezing

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45
Q

contraindications of roc

A

ypersensitivity

BURN patients

Immobilization- increased resistance

Acute Quadriplegic myopathy syndrome
In pt with corticosteroids

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46
Q

brand name of pancuronium

A

pavulon

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47
Q

classification of pancuronium

A

bisquaternary aminosteriod

non-depolarizing neuromuscular blocker

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48
Q

MOA of pancuronium

A

Long acting
Competitive antagonist with Ach at the nicotinic cholinergic receptors at the end plate of muscle. Binds to 1 alpha subunit of the post-synaptic receptor in a competitive fashioin.

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49
Q

use of pancuronium

A

Tracheal intubation
Immobility during surgery
Facilitate mechanical
Ventilation

50
Q

intubating dose of pancuronium

A
  1. 1 mg/kg

0. 08-0.12 mg/kg

51
Q

surgery dose of pancuronium

A

0.06-0.1 mg/kg

52
Q

maintenance dose of pancuronium

A

0.01mg/kg (60-100 minutes after first dose and then 0.01 mg.kg every 25-60 m ins

53
Q

continuous infusion dose of pancuronium

A

1-2 mcg/kg/min

54
Q

how much to reduce the pancuronium dose with renal failure

A

50% reduction with renal impairment

55
Q

onset of pancuronium

A

3-5 minutes

SLOW

56
Q

duration of pancuronium

A

60-120 minutes

57
Q

peak of pancuronium

A

3-5 minutes

58
Q

half life on pancuronium

A

110 minutes

59
Q

elimination of pancuronium

A

55-70% excreted in urine as unchanged drug

60
Q

metabolism of pancuronium

A

Hepatic 30 %-45%

Deacetylation to active metabolite 1/3-1/2 activity of parent drug

61
Q

adverse effects of pancuronium

A

CV: Vagolytic, increased HR, BP, CO

Derm: rash, itchy, erythema,burning in vein

GI- salivation

Neuro- muscle weakness

Resp- wheezing/bronchospasm

Hypersensitivity

62
Q

contraindications of pancuronium

A

Hypersensitivity

BURN patients

Immobilization- increased resistance

Acute Quadriplegic myopathy syndrome
In pt with corticosteroids

63
Q

brand name of mivacurium

A

mivacurium

64
Q

how is mivacurium supplied?

A

50 mg/ 5mL or 100 mg/10mL

10mg/1mL

65
Q

classification of mivacurium

A

bisquaternary benzylisoquinolinium

NDNMB

66
Q

MOA of mivacurium

A

Competitive antagonist
main site of action on nicotinic cholinergic receipts
at the end plate of muscle
binding site of Ach
some presynaptic receptor effect (release of ACh)
80-90% of receptors must be blocked to see reduction in twitch height

67
Q

use of mivacurium

A

tracheal intubation
immobility during surgery
facilitate mechanical ventilation

68
Q

intubation dose of mivacurium

A

0.25 mg/kg

69
Q

continuous infusion of mivacurium

A

3-15 mcg/kg/min

70
Q

onset of mivacurium

A

2-3 minutes

71
Q

peak of mivacurium

A

2-3 minutes

72
Q

duration of mivacurium

A

12-20 minutes

73
Q

half life of mivacurium

A

1-3 minutes

74
Q

metabolism of mivacurium

A

Hydolyzed by plasma cholinesterases at 80% the rate of Succs metabolism

Hydrolysis is concentration dependent

More drug = faster hydrolysis

75
Q

Adverse reactions with mivacurium

A

HISTAMINE → hypotension, tackycardia, bronchospasm

Caution in asthmatics

Hypotension more pronounced with hypertensive ptd

Pts with cholinesterase deficiency or reduced plasma cholinesterases

NO CV affect on cardiac muscarinic receptors (like pancuronium OR block ganglionic nicotinic receptors like d-tubocurine) so less hypotenion or tacky cardia but the histamine offsets these benefits

76
Q

contraindications with mivacurium

A

Atypical plasma cholinesterase patients → prolonged blockade

asthmatics

77
Q

what is a normal dibucane number?

A

80%

78
Q

what is a dibucane number of someone who is homozygous for atypical variant form of atypical plasma cholineserases

A

20%
20% of plasma cholinesterase was inhibited by admin of dibucaine
3 hours of blockade
mivacurium and pancuronium

79
Q

brand name of cisatracurium

A

nimbex

80
Q

how is cisatracurium supplied

A

10 mg/5mL
20 mg/10 mL
2mg/1mL

81
Q

classification of cisatracurium

A

intermediate acting
benzylisoquinolinium
NDNMB

82
Q

how much more potent is cisatracurium than atrracurium?

A

4x

83
Q

MOA of cisatracurium

A

Competitive antagonist
main site of action on nicotinic cholinergic receipts
at the end plate of muscle
binding site of Ach
some presynaptic receptor effect (release of ACh)
80-90% of receptors must be blocked to see reduction in twitch height

84
Q

use of cisatracurium

A

tracheal intubation
immobility during surgery
facilitate mechanical ventilation

85
Q

intubating dose of cisatracurium

A

0.15- 0.2 mg/kg

86
Q

dose of cisatracurium after succs is used to intubate

A

0.1 mg/kg

87
Q

maintenance dose of cisatracurium

A

0.03 mg/kg 40-60 minutes after initial dose

20 minute intervales

88
Q

infusion dose of cisatracurium

A

3mcg/kg/min
1-2mcg/kg/min
consider reduction of infusion by 30-40 % with volitiles

89
Q

onset of cisatracurium

A

2-3 min

90
Q

peak of cisatracurium

A

3-5 minutes

91
Q

duration of cisatracurium

A

20-35 minutes

92
Q

half life of cisatracurium

A

22-29 minutes

93
Q

metabolism of cisatracurium

A

NO ester hydrolysis

compared to atracurium

94
Q

elimination of cisatracurium

A

77% hoffman elimination
non-enzymatic base catalyzed reaction to spontaneous degradation at normal body temp and pH
16 % renal

95
Q

what accelerated hoffman elimination?

A

alkalosis

96
Q

what slow hoffman elimination?

A

acidosis and hypothermia

97
Q

how does the laundosine production compare between cisatracurium and atracurium?

A

cisatracurium is 5x less than atracuium

98
Q

adverse reaction with cisatracurium

A

RARE/MILD
histamine- suggestive
bradycardia

99
Q

contraindications with cisatracurium

A

Hypersensitivity

BURN patients

Immobilization- increased resistance

100
Q

conditions that antagonize NMB

LESS BLOCK

A
alkalosis
hypercalcemia
demyelinating lesions
peripheral neuropathies
denervation
infection
muscle trauma
DM
acetylcholinesterase inhibitors
burn injury 10 post injury peak 40 days decline 60 day
101
Q

conditions that potentiate NMB

MORE BLOCK

A
electrolyte abnormalities
severe hyponatremia
severe hypocalcemia
severe hypokalemia
hypermagnesemia
hypothemia
neuromuscular disease
acidosis
acute intermittent porphyria
eaton lambert syndrome
myasthenia gravis
calcium channel blockers
aminoglycosides( Gent, tobra)
inhalation anesthetics
lithium
magnesium  salts
procainamide
quinidine
loop diuretics
102
Q

brand name of atracurium

A

atracurium

103
Q

how is atracurium supplied

A

50 mg/5mL
100 mg/10mL
10mg/mL

104
Q

classification of atracurium

A

intermediate acting
bisquaternary benzylisoquinolinium
NDNMB
10 sterioisomers

105
Q

MOA of atracurium

A

Competitive antagonist
main site of action on nicotinic cholinergic receipts
at the end plate of muscle
binding site of Ach
some presynaptic receptor effect (release of ACh)
80-90% of receptors must be blocked to see reduction in twitch height

106
Q

use of atracurium

A

tracheal intubation
immobility during surgery
facilitate mechanical ventilation

107
Q

intubating dose of atracurium

A

0.4-0.5 mg/kg

108
Q

Maintenance dose of atracurium

A

0.08-0.1 mg/kg every 20-45 minutes initially then 15-25 minutes

109
Q

Initial dose after succ of atracurium

A

0.3-0.4 mg/kg

110
Q

Infusion dose of atracurium

A

9-10 mcg/kg/min (maintained at 5-9 mcg/kg/min

111
Q

ICU paralysis dose for atracurium

A

IV: bolus 0.4-0.5 mg/kg then 4-20 mcg/kg/min

112
Q

onset of atracurium

A

2-2.5 minutes

113
Q

duration of atracurium

A

20-35 min (95% recovery in 60-70 minutes)

114
Q

peak of atracurium

A

3-5 minutes

115
Q

half time of atracurium

A

2 minutes distribution to terminal 20 minues

116
Q

elimination of atracurium

A

Hoffman Elimination 1/3 non-enzymatic base catalyzed reaction leading to spontaneous degradation at normal body temp and pH

LAUNDANOSINE- not active at NMJ causes CNS stimulation

70% laudanosine is excreted in bile- biliary obstruction can lead to accumulation of the metabolite

117
Q

what does laundanosine cause as a metabolite of atracurium

A

Increased volatile requirement

Vasodilation

118
Q

metabolism of atracurium

A

Hydrolysis by non-specific plasma esterases 2/3
Laundosin is the metabolite for both ester hydrolysis and Hoffman

Non-renal/hepatic

119
Q

adverse reactions of atracurium

A

Mild/RARE

Flushing

Increase HR decrease MAP 5 min recovery

Facial and truncal flushing

Bradycardia

0.5 mg/kg

120
Q

contraindications with atracurium

A

AVOID WITH ASTHMATICS

Burns

Immobilization

Hypersensitivity/ anaphylactic

121
Q

typical dose with atracurium

A
50 mg for intubation 
may need more if big male
need to re-dose after 30 minutes
usually about 10-20 mg
lasts 30 minutes
takes 2 minutes to get on board